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Drug, Bio-affecting And Body Treating Compositions > Designated Organic Active Ingredient Containing (doai) > Peptide Containing (e.g., Protein, Peptones, Fibrinogen, Etc.) Doai > Cyclopeptides

Cyclopeptides

Cyclopeptides patent applications listed are from June 2005 to current and include Date, Patent Application Number, Patent Title, Patent Abstract summary and are linked to the corresponding patent application page.

02/15/07 - 20070037738 - Using inhibitors of histone deacetylases for the suppression therapy of inherited disease predisposing conditions
Compounds can be used to act as inhibitors of enzymes having histone deacetylase activity for the medical therapy of conditions which predispose a person for the development of a disease, such as but not limited to cancer, inflammatory or metabolic diseases. Such conditions are linked to genetically inherited mutations of ...

02/08/07 - 20070032411 - Protein kinase signalling
The present invention provides a method of selecting or designing a compound for the ability to regulate JAK activity. The method comprises assessing the ability of the compound to modulate the interaction of the pseudo-substrate loop (PSL) with the kinase like domain (KLD) of JAK. In addition the present invention ...

02/08/07 - 20070032410 - Compositions and methods for the treatment of psychiatric disorders
Methods and compositions containing oxytocin or an oxytocin analog, specifically carbetocin, are provided for the prevention and treatment of autism spectrum disorders, related disorders and symptoms of such disorders. The methods and compositions of the invention are effective in the treatment of social withdrawal, eye contact avoidance, repetitive behaviors, anxiety, ...

02/08/07 - 20070032409 - Bradykinin receptor antagonists and uses thereof
The present invention regards bradykinin receptor antagonists for treatment of a medical condition. In particular, the medical condition follows cardiopulmonary bypass. In specific embodiments, bradykinin receptor antagonists are used for the treatment of protamine-induced hypotension and/or fibrinolysis. ...

02/08/07 - 20070032408 - Novel spacer moiety for poly (ethylene glycol) modified peptide based compounds
wherein α, β, γ, δ, and ε are each integers whose values are independently selected. ...

02/01/07 - 20070027071 - Hcv ns3 protease inhibitors
The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections. ...

02/01/07 - 20070027070 - Medicinal uses of mu-opioid receptor agonists
The present invention provides methods for stimulating mu-opioid receptors with agonist peptides in a mammal in need thereof. The methods comprise administering to the mammal an effective amount of a selective mu-opioid receptor agonist peptide that comprises at least two α-amino acid residues. At least one of the amino acid ...

01/25/07 - 20070021331 - Methods of using macrocyclic modulators of the ghrelin receptor
The present invention provides novel conformationally-defined macrocyclic compounds that have been demonstrated to be selective modulators of the ghrelin receptor (growth hormone secretagogue receptor, GHS-R1a and subtypes, isoforms and variants thereof). Methods of synthesizing the novel compounds are also described herein. These compounds are useful as agonists of the ghrelin ...

01/25/07 - 20070021330 - Aza-peptide macrocyclic hepatitis c serine protease inhibitors
The present invention relates to compounds of Formula (I), or a pharmaceutically acceptable salt, ester, or prodrug, thereof, which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus ...

01/25/07 - 20070021329 - Treatment of hypersensitivity conditions
This invention relates to methods of treatment of hypersensitivity conditions such as asthma and other allergic conditions, and especially to treatment of these conditions with cyclic peptidic and peptidomimetic compounds which have the ability to modulate the activity of G protein-coupled receptors. The compounds preferably act as antagonists of the ...

01/11/07 - 20070010431 - Pharmaceutical formulations and methods of treatment using the same
Pharmaceutical formulations containing at least one compound of Formulae I-XXVI herein and at least one surfactant. Pharmaceutically acceptable carriers and excipients may also be included in the formulations. The formulations of the present invention are suited for use in single unit dosages. ...

01/04/07 - 20070004619 - Relaxin superfamily peptide analogues
Monomeric, cyclic peptide analogues of relaxin superfamily proteins, based on B-chains of relaxin superfamily proteins, and methods of making them, are described, as well as pharmaceutical compositions containing them and methods of utilising them. ...

12/28/06 - 20060293224 - Conformationally stabilized cell adhesion peptides
Novel synthetic Arg-Gly-Asp containing peptides which have high affinity and specificity for their receptors by virtue of restrictions on their stereochemical conformation. Such restrictions can be provided by cyclization, by inclusion into a constraining conformational structure such as a helix, by providing an additional chemical structure such as an amide ...

12/28/06 - 20060293223 - Uses of melanocortin-3 receptor (mc3r) agonist peptides
The present invention provides methods of treating metabolic disorders, including, for example, obesity, diabetes mellitus, cachexia, sarcopenia, and cardiovascular disorders, methods of inducing weight loss and increasing muscle mass in a patient, by administration of MC3R agonist peptides. Furthermore, the present invention provides the use of an MC3R agonist peptide ...

12/21/06 - 20060287225 - Integrin inhibitors for the treatment of eye diseases
Methods and compositions for prophylaxis and/or treatment of diseases of the eye using antagonists of the integin receptors αvβ3 and/or αvβ5. The compositions can be nanoparticles and are administered to the eye by injection into the vitreous body of the eye. ...

12/14/06 - 20060281670 - Compositions and methods for modulating angiogenesis
Methods and compositions for modulating angiogenesis are disclosed. Such modulation is made possible by the use of NK-B, NK-B analogs, NK receptor agonists and NK receptor antagonists to promote or inhibit angiogenesis. The method for modulating the angiogenic activity of cells comprises contacting cells capable of angiogenesis with an effective ...

12/07/06 - 20060276379 - Binding peptides specific for the extracellular domain of erbb2 and uses therefor
The invention provides methods and compositions for diagnosing and treating subjects using EBPs. Specifically disclosed are peptides and peptidomimetics that bind selectively to the extracellular domain of ErbB2. These compositions are useful in the prevention and treatment of disorders characterized by ErbB2 overexpression (e.g., breast cancer). ...

11/23/06 - 20060264358 - Acylated nonadepsipeptides ii
The invention relates to nonadepsipeptides and processes for their preparation, and to their use for producing medicaments for the treatment and/or prophylaxis of diseases, in particular bacterial infectious diseases. ...

11/16/06 - 20060258573 - Peptide anti-tumor agent
Disclosed herein are isolated, purified peptides, biologically active fragments and analogs of the peptides having anti-tumor activity in mammals, pharmaceutical formulations comprising the peptides, fragments and analogs and methods of treating mammals suffering from tumors using such materials. ...

11/16/06 - 20060258572 - Somatostatin-dopamine chimeric analogs
The invention features somatostatin-dopamine chimeric analogs and methods relating to their therapeutic use for the treatment of neoplasia, acromegaly, and other conditions. ...

11/16/06 - 20060258571 - Antibacterial ester macrocycles
The invention relates to antibacterial ester macrocycles of formula (I), methods for the production thereof, and the use thereof for producing medicaments used for the treatment and/or prophylaxis of diseases, particularly bacterial infections. ...

11/09/06 - 20060252673 - Histogranin-like peptides and non-peptides, processes for their preparation and uses thereof
R4 and R5 are, independent of one another, -hydrogen, —(C1-C6)alkyl, -methyloxy, -nitro, -amino, -arylcarbonylamino, —(C1-C6)alkoylamino, —(C1-C6)alkylamino, -halo or —OH. ...

11/02/06 - 20060247157 - Methods for making intermediates and oxytocin analogues
More efficient and/or economical methods for synthesizing heptapeptide alcohol analogs of oxytocin are provided along with novel intermediates which are useful in synthesizing such oxytocin analogs. Efficient and economical methods for synthesizing intermediates useful in synthesizing these oxytocin analogs are also provided. ...

11/02/06 - 20060247156 - Use of neuropeptides for ligament, cartilage, and bone healing
Disclosed are a method and a corresponding pharmaceutical composition for treating damaged cartilage and subchondral bone. Neurogenic compounds in general and neuropeptides in particular have been found to be highly effective in stimulated repair of cartilage and bone damaged due to traumatic injury, ligament disease, and disuse. Preferred active ingredients ...

10/26/06 - 20060241026 - Novel cyclic peptides and use thereof as anti-microbial agents
The invention relates to compounds selected from: peptides having formula (1): C(s)—X1—X2—X3—X4—X5—X6—X7-C(s), wherein the two cysteine residues are linked by means of a disulphide bridge which is represented by symbol C(s) and X1, X2, X3X4, X5, X6 and X7 denote amino acids selected from a determined list; and derivatives of ...

10/19/06 - 20060234923 - Template-fixed peptidomimetics as medicaments against hiv and cancer
Template-fixed β-hairpin peptidomimetics of the General Formula (I); wherein Z1 and Z2 are template-fixed chains of 4 and 6 or 5 and 7 α-amino acid residues which, depending on their positions in the chain are Gly, or Pro, or of certain types which, as the remaining symbols in the above ...

10/19/06 - 20060234922 - Remedy for corneal failure
The present invention provides a new type of pharmaceutical agent that recovers corneal sensitivity after corneal surgery or improves the condition of dry eye. Application of a somatostatin receptor agonist is expected to provide an improvement effect on decreased corneal sensitivity after cataract surgery or LASIK surgery, decreased corneal sensitivity ...

10/19/06 - 20060234921 - Treatment of osteoarthritis
This invention relates to methods of treatment of osteoarthritis, and especially to treatment of this condition with cyclic peptidic and peptidomimetic compounds which have the ability to modulate the activity of G protein-coupled receptors. The compounds preferably act as antagonists of the C5a receptor, and are active against C5a receptors ...

10/19/06 - 20060234920 - New antitumoral compounds
The present invention is directed to new kahalalide antitumoral compounds, in particular to analogues of kahalalide F, useful as antitumoral, antiviral, antifungal agents and in the treatment of psoriasis. ...

10/19/06 - 20060234919 - Use
The present invention relates to the use of substances with oxytocin for the preparation of pharmaceutical composition against inflamation. It also relates to a pharmaceutical composition comprising at least one substance with oxytocin activity against inflamation. ...

10/12/06 - 20060229238 - Sustained release of microcrystalline peptide suspensions
The invention relates to a fluid, milky microcrystalline aqueous suspension of a peptide or peptidomimetic and a counter-ion of a strong proton donor in water, wherein the peptide or peptidomimetic and counter-ion are present in amounts and at a molar ratio sufficient to form the suspension upon mixing and without ...

10/12/06 - 20060229237 - Treatment of gastrointestinal distress
A composition and method for treating and/or preventing acute and chronic gastrointestinal distress including nausea, vomiting, lactose intolerance, obstructive symptoms, diarrhea, mucositis, bleeding, weight loss, and malnutrition in a subject who is immunocompromised or receives a planned course of chemotherapy and/or radiotherapy. The method comprises administering a histone deacetylase inhibitor ...

10/12/06 - 20060229236 - Cyclic tetrapeptide compound and use thereof
A cyclic tetrapeptide compound of the formula (I): wherein R1 is hydrogen; R2 is lower alkyl, aryl, optionally substituted ar(lower)alkyl, heterocyclic(lower)alkyl, cyclo(lower)alkyl(lower)alkyl, lower alkylcarbamoyl(lower)alkyl or arylcarbamoyl(lower)alkyl; R3 and R4 are each independently hydrogen, lower alkyl, optionally substituted ar(lower)alkyl, optionally substituted heterocyclic(lower)alkyl or cyclo(lower)alkyl(lower)alkyl, or R3 and R4 are linked together ...

10/05/06 - 20060223746 - Methods and compositions for the treatment of diseases of the eye
Methods and compositions for prophylaxis and/or treatment of diseases of the eye of a patient resulting angiogenesis in the eye using antagonists of the integrin receptors αvβ3 and/or αvβ5. The compositions can be nanoparticles and are administered to the eye by injection into the sclera of the eye. ...

10/05/06 - 20060223745 - Macrocyclic compounds having aspartic protease inhibiting activity and pharmaceutical uses thereof
The present invention relates to macrocyclic compounds of formula (I), wherein R1, is (C1-8)alkyl, (C1-4)alkoxy(C1-4)alkyl, hydroxy(C1-6)alkyl, (C1-4)alkylthio(C1-4)alkyl, (C1-6)alkenyl, (C3-7)cycloalkyl, (C3-7)cycloalkyl(C1-4)alkyl, piperidinyl or pyrrolidinyl, R2 and R4, independently, are hydrogen or optionally substituted (C1-8)alkyl, (C3-7)cycloalkyl, (C3-7)cycloalkyl(C1-4)alkyl, aryl, aryl(C1-4)alkyl, heteroaryl or heteroaryl(C1-4)alkyl, or R2 and R4, together with the nitrogen to which ...

09/28/06 - 20060217294 - Compounds binding to p-selectin
The present invention relates to derivatives of compounds which bind selectively to the adhesion molecule human P-selectin, and particularly to such derivatives which comprise a peptide moiety or a functional equivalent of said peptide moiety and are represented by X(Ax)mA3A1A2A1Y. In addition, the invention relates to methods for preparing such ...

09/21/06 - 20060211607 - Somatostatin-dopamine chimeric analogs
Disclosed is a series of somatostatin-dopamine chimeric analogs which retain both somatostatin and dopamine activity in vivo. An example is: 6-n-propyl-8β-ergolinglmethylthioacetyl-D-Phe-c(Cys-Tyr-D-Trp-Lys-Abu-Cys)-Thr-NH2 ...

09/21/06 - 20060211606 - Peptides
This invention relates to biologically active polypeptides derived from the E peptide that forms the C-terminus of the insulin-like growth factor I (IGF-I) splice variant known as mechano growth factor (MGF). These peptides are modified to improve their stability compared to the naturally occurring E peptide. ...

09/14/06 - 20060205638 - Process for preparing macrocyclic compounds
The compounds of formula (I) are potent active agents for the treatment of hepatitis C virus (HCV) infection. ...

09/14/06 - 20060205637 - Fluoro-alkyl-cyclopeptide derivatives having anti-integrin activity
Compounds of formula (I) cyclo [NX1-R1-CO—NX2-R2-CO—NX3-R3-CO—NX4-CO—NX5-R5-CO], wherein at least one x-fluoroalkylated amino acid is present, are inhibitors of integrins, particularly those belonging to the alphavbeta3 and alphavbeta5 family, and thus are useful as medicaments, particularly for the treatment of the underlying diseases responsible for abnormal angiogenesis, such as retinopathy, acute ...

09/14/06 - 20060205636 - Oxytocin as cardiomyogenesis inducer and uses thereof
The invention relates to oxytocin and oxytocin-related compounds and functional derivatives thereof, and uses thereof to induce differentiation of a non-cardiomyocyte (e.g. a stem/progenitor cell) to a cardiomyocyte. The invention further relates to the methods of prevention or treatment of conditions characterized by or associated with a cardiomyocyte loss or ...

08/17/06 - 20060183673 - Antibiotic 107891, its factors a1 and a2, pharmaceutically acceptable salts and compositions, and use thereof
Antibiotic 107891 and its Factors A1 and A2 show a good antibacterial activity against Gram-positive bacteria including methicillin resistant and vancomycin resistant strains, and is active also against some Gram-negative bacteria such as M. catharralis, Neisseria species and H. influenzae and Mycobacteria. ...

07/27/06 - 20060166869 - Novel use of lipopeptide preparations
The invention relates to the use of lipopeptide preparations as anti-tilted-peptide agents, which are able to inhibit or limit the destabilization effect of tilted peptides on hydrophobic/hydrophilic interfaces, for instance on membranes. The lipopeptides include surfactins, iturins, and fengycins. The invention also relates to a process for the production of ...

07/27/06 - 20060166868 - Vegf peptides and their use
A novel peptide having the amino acid sequence SCKNTDSRCKARQLELNERTCRCDKPRR or a fragment thereof that substantially retains NP-1 antagonist activity, in cyclic form, is proposed for use in therapy. ...

07/20/06 - 20060160726 - Cyclic agonists and antagonists of c5a receptors and g protein-coupled receptors
The present invention relates to novel cyclic or constrained acyclic compounds which modulate the activity of G protein-coupled receptors and are useful in the treatment of conditions mediated by G protein-coupled receptors, for example, inflammatory conditions. ...

07/13/06 - 20060154857 - Compositions for down-regulation of ccr5 expression and methods of use thereof
The present invention relates to the downregulation of surface receptor CCR5 expression through manipulation of the cell cycle in activated lymphocytes by administering a composition that arrests the G1 phase of the cell cycle, thereby reducing receptor sites for entry of HIV into T cells, and thus, the effects of ...

07/13/06 - 20060154856 - Nadph oxidase inhibition pharmacotherapies for obstructive sleep apnea syndrome and its associated morbidities
The invention relates to compositions and methods for treating Obstructive Sleep Apnea (OSA). Specifically, the invention relates to the use of NADPH Oxigenase inhibitors in compositions and methods for treating OSA in a subject. ...

07/06/06 - 20060148685 - Use of substances with oxytocin activity against climacteric disorders
The present invention relates to the use of substances with oxytocin activity against climacteric disorders or similar symptoms due to dysfunction in the ovaries. It also relates to a pharmaceutical composition comprising at least one substance with oxytocin activity against climacteric disorders. ...

07/06/06 - 20060148684 - Use of a histone deacetylase inhibitor for treating muscular dystrophies
The invention relates to an inhibiter of histone deacetylase for treating or preventing a disease resulting from the deficiency of an adult gene in an individual by the re-expression of the homologous fetal gene. The invention concerns in particular the treatment of dystrophies such as Duchenne's dystrophy or Becker's dystrophy ...

07/06/06 - 20060148683 - Detection and treatment of intravascular lesions
Optical agents that contain a fibrin binding moiety covalently linked to an optical dye are described, as well as methods of treating intravascular lesions in a patient using such optical agents. ...

06/22/06 - 20060135412 - Methods for the treatment of alzheimers disease and compositions therefore
The invention discloses previously unknown modifiers of Aβ secretion. These proteins are identified as suitable targets for the development of new therapeutics to treat, prevent or ameliorate pathological conditions associated with Aβ secretion, including Alzheimer's Disease. The invention also relates to methods to treat, prevent or ameliorate said pathological conditions ...

06/22/06 - 20060135411 - Treatment of inflammatory bowel disease
This invention relates to methods of treatment of inflammatory bowel disease, and especially to treatment of this condition with cyclic peptidic and peptidomimetic compounds which have the ability to modulate the activity of G protein-coupled receptors. The compounds preferably act as antagonists of the C5a receptor, and are active against ...

06/15/06 - 20060128614 - Antimicrobial peptides with reduced hemolysis and methods of their use
The present invention provides novel cyclic and linear short peptides containing one of the following amino acid residue sequences: Xa1-Naa-Xa1-Xa1-Naa-Xa2 or Xa1-Naa-Xa2-Xa1-Naa-Xa1 wherein: Xa1 represents lysine, arginine, or histidine; Naa represents an unnatural hydrophobic aromatic amino acid moiety selected from the group consisting of (naphtha-1-yl)alanine (1-Nal), (naphtha-2-yl)alanine (2-Nal), (benzothien-3-yl)alanine (Bal), ...

06/15/06 - 20060128613 - Melanocortin receptor ligands
wherein R2, R4, R4′, R5, R6, R6′, R7, R8, R8′, R9, R9′, R10, Ar, Z1, Z2, Z3, X, B, D, p, q, r and s are as described in the specification and claims, and optical isomers, diastereomers or enantiomers thereof; pharmaceutically-acceptable salts, hydrates, and biohydrolyzable esters, amides or imides thereof. ...

06/08/06 - 20060122103 - Dalfopristine/quinupristine combinations with cefpirome
A pharmaceutical composition comprising synergistically effective amounts of cefpirome and dalfopristine/quinupristine combination. A method of treating a patient comprising the administration of synergistically effective amounts of cefpirome and a dalfopristine/quinupristine combination. Kits comprising synergistically effective amounts of cefpirome and a dalfopristine/quinupristine combination are also disclosed. ...

06/01/06 - 20060116316 - Heterocyclic inhibitors of ires-mediated translation and methods of use thereof
The present invention provides heterocyclic compounds that exhibits IRES-inhibitory activity. The heterocyclic compounds generally a nine-membered ring of three repeating C—C—N subunits covalently bound through amide bonds, and variable side groups linked to a central carbon of each subunit. Formulations and kits containing the subject compounds are also provided. ...

05/25/06 - 20060111281 - Cyclic peptide compositions for treatment of sexual dysfunction
or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, m and p are as defined. Further provided are compositions for treatment of sexual dysfunction in mammals, including male sexual dysfunction, such as erectile dysfunction, and female sexual dysfunction, by administration of a cyclic peptide including a ...

05/25/06 - 20060111280 - Novel substance fki-1033 and process for producing the same
in a medium, accumulating FKI-1033 substance in the cultured medium, and isolating FKI-1033 substance from the cultured mass. The thus obtained FKI-1033 substance has ryanodine binding inhibition activity, insecticidal activity and anthelmintic activity, and is expected as useful drugs as agrochemicals, veterinary drugs and medicaments in effectiveness and toxicity. ...

05/18/06 - 20060105943 - Cyclic peptidomimetic urokinase receptor antagonists
The present invention relates to cyclic peptides as inhibitors of urokinase binding to the urokinase receptor. Said cyclic peptides are suitable as pharmaceutical active substances for disorders mediated by urokinase and its receptor. ...

05/18/06 - 20060105942 - Inhibition of cell division based use of analogs of neuropeptide y
We describe peptides with cell-cycle inhibitory and anti-angiogenic activity and their use in the treatment of diseases which would benefit from the inhibition of cell division and/or angiogenesis, for example cancer. ...

05/11/06 - 20060100141 - Anti-allergic complex molecules
The present invention discloses novel anti-allergic complex molecules, and in particular, peptidic or peptidomimetic molecules, that includes a first part which is competent for cell penetration and a second part which is able to reduce or abolish mast cell degranulation, in particular to reduce or abolish allergy mediators, including histamine ...

05/11/06 - 20060100140 - Combination of a) n-{5-[4-(4-methyl-piperazino-methyl)-benzoylamido]2-methylphenyl}-4- (3-pyridyl)-2-pyrimidine-amine and b) a histone deacetylase inhibitor for the treatment of leukemia
The invention pertains to a combination of a histone deacetylase inhibitor and N-{5-[4-(4-methyl-piperazino-methyl)-benzoylamido]-2-methylphenyl}-4-(3-pyridyl)-2-pyrimidine or a pharmaceutically acceptable salt thereof for simultaneous, separate or sequential use for the treatment of leukemia and especially N-{5-[4-(4-methyl-piperazino-methyl)-benzoylamido]-2-methylphenyl}-4-(3-pyridyl)-2-pyrimidine-resistant leukemia. ...

05/04/06 - 20060094644 - Capreomycin derivatives and their use as antibacterials
The present subject matter relates to phenylurea capreomycin derivatives, and to metabolites and pharmaceutically acceptable salts and solvates thereof. The compounds of the present subject matter are useful as antibacterial agents for treating bacterial infections and for treating disorders caused by bacterial infections. The present subject matter also relates to ...

04/27/06 - 20060089300 - Macrocyclic peptides active against the hepatitis c virus
wherein R1 is (C1-8)alkyl, (C3-7)cycloalkyl, {(C1-6)alkyl-(C3-7)cycloalkyl} or Het, which are all optionally substituted from 1 to 3 times with halo, cyano, nitro, O—(C1-6)alkyl, amido, amino or phenyl, or R1 is C6 or C10 aryl which is optionally substituted from 1 to 3 times with halo, cyano, nitro, (C1-6)alkyl, O—(C1-6)alkyl, amido, ...

04/27/06 - 20060089299 - Selective treatment of endothelial somatostatin receptors
The invention provides for the use of somatostatin receptor selective ligands (selective for SSTR1 or SSTR4) to treat human endothelial cells and to formulate medicaments for human use. The medicaments may for example be used to treat an angiogenic disease. In various embodiments, the angiogenic disease may for example be ...

04/27/06 - 20060089298 - Novel substances k01-b0171 and process for producing the same
The present invention is comprised of culturing a microorganism having ability to produce K01-B0171-B substance and/or K01-B0171-C substance in a medium, accumulating K01-B0171-B substance and/or K01-B0171-C substance in a culture fluid and isolating K01-B0171-B substance and/or, K01-B0171-C substance from the culture fluid. The obtained K01-B0171-B substance, K01-B0171-C substance or a ...

03/30/06 - 20060069017 - Somatostatin analog and uses thereof
or a pharmaceutically acceptable salt thereof, and uses thereof. ...

03/30/06 - 20060069016 - Cyclosporin alkyne analogues and their pharmaceutical uses
with X, R0, R1, and R2 defined herein. ...

03/30/06 - 20060069015 - Novel cyclosporin analogues and their pharmaceutical uses
with X, R0, R1, and R2 defined herein. ...

03/30/06 - 20060069014 - Inhibition of histone deacetylase as a treatment for cardiac hypertrophy
The present invention provides for methods of treating and preventing cardiac hypertrophy. Class II HDACs, which are known to participate in regulation of chromatin structure and gene expression, have been shown to have beneficial effects on cardiac hypertrophy. Surprisingly, the present invention demonstrates that HDAC inhibitors inhibit cardiac hypertrophy by ...

03/23/06 - 20060063708 - Composition and method for regulation of body weight and associated conditions
Methods for regulating body weight and/or regulating weight gain are provided herein. The methods are useful, for instance, for treating or preventing obesity. Specifically, methods of administering varying levels of various alpha melanocyte stimulating hormone (α-MSH) analog compounds to an animal are provided for reducing body weight and/or reducing the ...

03/09/06 - 20060052289 - Use of somatostatin analogs in sleep apnea
Somatostatin analogues, e.g. comprising an amino acid sequence of formula -(D/L)Trp-Lys-X1-X2- wherein each of X1, and X2 is an amino acid residue as disclosed in the specification, have interesting properties in the treatment of sleep apnea. ...

02/23/06 - 20060040858 - Novel peptides that bind to the erythropoietin receptor
The present invention relates to peptide compounds that are agonists of the erythropoietin receptor (EPO-R). The invention also relates to therapeutic methods using such peptide compounds to treat disorders associated with insufficient or defective red blood cell production. Pharmaceutical compositions, which comprise the peptide compounds of the invention, are also ...

02/23/06 - 20060040857 - 1-desamino-8-a-arginyl vasopressin analogs
wherein, X is an amino acid of the group consisting of alanine, asparagine, glutamine, isoleucine, leucine and valine; and is an amino acid of the group consisting of asparagine, glutamine, isoleucine, leucine and valine. ...

// - 2. Analogs of 1-desamino-8-D-arginyl vasopressin, as claim 1, with the following general formula: -
...

// - 1. Analogs of 1-desamino-8-D-arginyl vasopressin with the following general formula: -
...

02/16/06 - 20060035820 - New derivatives of echinocandine, their preparation process and their use as antifungals
Z: H, CH3. The compounds of formula (I) have antifungal properties. ...

02/16/06 - 20060035819 - Novel molecule
The present invention relates generally to a molecular framework having a cyclic structure. More particularly, the present invention provides cyclic proteins and derivatives thereof in which particular turns and other elements of the molecular structure are held in defined orientations with respect to each other. The cyclic proteins of the ...

01/26/06 - 20060019883 - Use of cyclin d1 inhibitors
The present invention relates to use of certain cyclin D1 inhibitors at the manufacture of pharmaceutical preparations to be used in the treatment of patients to improve their response to tamoxifen treatment following a breast cancer treatment, either surgically, using cytotoxic compounds and/or irradiation, as well as a method of ...

01/19/06 - 20060014676 - Cyclic peptides for treatment of cachexia
where R1, R2, R3, R4a, R4b, R5, R6, R7, x, y and z are as defined in the specification, and a method of treating body weight disorders, including cachexia, sarcopenia and wasting syndrome or disease, and treating inflammation and immune disorders. ...

01/19/06 - 20060014675 - Methods for preparing internally constrained peptides and peptidomimetics
The present invention relates to a method for preparing a peptide having a stable, internally constrained alpha-helical, beta-sheet/beta-turn, 310-helical, or pi-helical region and a method of stabilizing an alpha-helical, beta-sheet/beta-turn, 310-helical, or pi-helical region within a peptide structure. The resulting peptides and methods of using them are also disclosed. ...

01/19/06 - 20060014674 - Methods for preparing purified lipopeptides
The present invention relates to crystalline and crystal-like forms of lipopeptides, including daptomycin, a lipopeptide antibiotic with potent bactericidal activity against gram-positive bacteria, including strains that are resistant to conventional antibiotics. The present invention relates to methods of purifying lipopeptides, including daptomycin, a lipopeptide antibiotic with potent bactericidal activity against ...

01/05/06 - 20060003926 - Pharmaceuticals for the imaging of angiogenic disorders
useful for the diagnosis and treatment of cancer, methods of imaging tumors in a patient, and methods of treating cancer in a patient. The present invention also provides novel compounds useful for monitoring therapeutic angiogenesis treatment and destruction of new angiogenic vasculature. The pharmaceuticals are comprised of a targeting moiety ...

12/29/05 - 20050288221 - Glycopeptide antibiotics
Wherein R1, R2, R3, R4, R5, R6a, R6b, R6c, R6d, R6e and R7 are defined in the specification. These compounds are useful as antibiotic agents. ...

12/15/05 - 20050277583 - Histone deacetylase inhibitors and process for producing the same
Compounds represented by formula (1) have strong inhibitory activity that is selective towards HDAC1 and HDAC4. Therefore, the compounds of the present invention are useful as pharmaceutical agents for treating or preventing diseases caused by HDAC1 and HDAC4. ...

12/08/05 - 20050272646 - Streptogramin antibiotics
Disclosed is a cyclic peptide antibiotic in which an enzyme-sensitive bond is replaced by an enzyme-resistant bond. ...

12/08/05 - 20050272645 - Retrocyclins: antiviral and antimicrobial peptides
Retrocyclin peptides are small antimicrobial agents with potent activity against bacteria and viruses. The peptides are nonhemolytic, and exhibit minimal in vitro cytotoxicity. A pharmaceutical composition comprising retrocyclin as an active agent is administered therapeutically to a patient suffering from a bacterial and/or viral infection, or to an individual facing ...

12/08/05 - 20050272644 - Method for increasing therapeutic gain in radiotherapy and chemotherapy
The present invention provides compositions and methods for increasing therapeutic gain in radiotherapy and chemotherapy for proliferating malignant or nonmalignant disease to produce high probability of tumor control with low frequency of sequelae of therapy by administering a therapeutically effective amount of a histone deacetylase inhibitor. The compounds are capable ...

12/01/05 - 20050267019 - Echinocandin derivatives, their method of preparation and their application as anti-fungal agents
wherein the substituents are as defined in the application useful as antifungal agents. ...

12/01/05 - 20050267018 - Macrocyclic compounds as inhibitors of viral replication
The embodiments provide compounds of the general formulas I-XIX, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating flaviviral infection, including hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an ...

12/01/05 - 20050267017 - Conformationally constrained c-backbone cyclic peptides
Backbone cyclized peptide analogs that include at least one building unit of a Cα(ω-functionalized) amino acid that is constructed to include a spacer and a terminal functional group. The bridging groups are attached via alpha carbons of amino acid derivatives to provide novel non-peptide linkages. Also disclosed are novel Cα(ω-functionalized) ...

11/24/05 - 20050261173 - Antifungal parenteral products
Parenteral pharmaceutical formulations containing an echinocandin antifungal compound and an aqueous solvent are provided, wherein the formulation includes ethanol, for example about 20% w/v ethanol. The parenteral pharmaceutical formulation may further include one or more additives, such as a stabilizing agent, buffer or tonicity agent. The parenteral pharmaceutical formulations are ...

11/17/05 - 20050256037 - Antibacterial amide macrocyles
The invention relates to antibacterial amide macrocycles and process for their preparation, their use for the treatment and/or prophylaxis of diseases, and to their use for producing medicaments for the treatment and/or prophylaxis of diseases, especially of bacterial infections. ...

11/10/05 - 20050250682 - Treatment of membrane-associated diseases and disorders using lantibiotic containing compositions
Compositions useful for treating membrane-associated diseases, conditions, and disorders, including inflammatory diseases, dry mouth, primary ciliary dyskinesia and platelet aggregating disorders, are disclosed which comprise at least one lantibiotic compound. Also disclosed are pharmaceutical compositions and methods of treatment for membrane-associated diseases such as inflammation and dermal irritation, as well ...

11/10/05 - 20050250681 - Treatment of ocular diseases and disorders using lantibiotic compositions
Compositions and methods for treating ocular diseases and disorders are provided. The composition can contain at least one lantibiotic, which can be administered topically by injection, systemically, or by other appropriate means. The methods provided include the administration of a therapeutically effective amount of a formulation containing at least one ...

11/10/05 - 20050250680 - Stabilized alpha helical peptides and uses thereof
Novel polypeptides and methods of making and using the same are described herein. The polypeptides include cross-linking (“hydrocarbon stapling”) moieties to provide a tether between two amino acid moieties, which constrains the secondary structure of the polypeptide. The polypeptides described herein can be used to treat diseases characterized by excessive ...

11/03/05 - 20050245439 - Prevention of joint destruction
A method for treating, preventing or reducing the risk of joint destruction in a subject who suffers from a joint or musculoskeletal disease. The method comprises administering a histone deacetylase (HDAC) inhibitor or in conjunction with other agents to inhibit degradation and resorption of cartilage and bone in the joint. ...

11/03/05 - 20050245438 - Receptor(sstr4)-selective somatostatin analogs
Analogs of SRIF which are selective for SSTR4 in contrast to the other cloned SRIF receptors are useful in determining tissue and cellular expression of the receptor SSTR4 and its biological role in regulating tumor growth. SRIF analog peptides, such as des-AA1,2,4,5,12,13[Ala7]-SRIF; des-AA1,2,4,5,12,13[Aph7]-SRIF, des-AA1,2,4,5,12,13[Aph7]Cbm-SRIF; des-AA1,2,4,5,12,13[Tyr2,Ala7]-Cbm-SRIF, and des-AA1,2,4,5,12,13[Tyr7,CβMe-L-2Nal8]-SRIF, and counterparts incorporating ...

11/03/05 - 20050245437 - Peptides having antimicrobial properties and compositions containing them, notably for the preservation of foodstuffs
having antimicrobial properties and compositions containing them, notably for the preservation of foodstuffs. ...

10/27/05 - 20050239695 - Process for the formation of disulfide bonds in cyclic peptides
A non-oxidative process is described for the formation of an intramolecular disulfide bond in precursors of the peptide or peptidomimetic type; said process comprises the preparation of a linear intermediate containing an —SH group in the S-sulfonate form and a second —SH group which is obtainable in the free form ...

10/27/05 - 20050239694 - Cyclic depsipeptide as chemotherapeutic anticancer agent
Serratamolide, also named cyclo[(3R)-3-hydroxydecanoyl-L-seryl-(3R)-3-hydroxydecanoyl-L-seryl], is a cyclic depsipeptide isolated from cultures of bacteria of the species Serratia marcescens. Serratamolide decreases the viability of, and induces apoptosis in several cancer cells (leukemias, myelomas, carcinomas, etc.), virtually with no effect on non-cancer cells. This makes serratamolide, and its pharmaceutically acceptable addition salts ...

10/27/05 - 20050239693 - Template-fixed peptidomimetics with antibacterial activity
wherein Z is a template-fixed chain of 12 α-amino acid residues which, depending on their positions in the chain (counted starting from the N-terminal amino acid) are Gly, or Pro, or of certain types which, as the remaining symbols in the above formula, are defined in the description and the ...

10/27/05 - 20050239692 - Aqueous preparation containing oligopeptides and etherified cyclodextrin
The present invention relates to an aqueous pharmaceutical preparation of oligopeptides comprising an oligopeptide of the formula I, cyclo-(n-Arg-nGly-nAsp-nD-nE), and a partially etherified β-cyclodextrin having a water solubility of greater than 1.8 mg/ml of water, and to the preparation of the aqueous pharmaceutical preparation. ...

10/20/05 - 20050233953 - Histogranin-like peptides, processes for their preparation and uses thereof
R4 and R5 are, independent of one another, -hydrogen, —(C1-C6)alkyl, -methyloxy, -nitro, -amino, -arylcarbonylamino, —(C1-C6)alkoylamino, —(C1-C6)alkylamino, -halo or —OH. ...

10/20/05 - 20050233952 - Antibiotic 107891, its factors a1 and a2, pharmaceutically acceptable salts and compositions, and use thereof
The invention relates to an antibiotic substance of microbial origin, arbitrarily denominated antibiotic 107891 which is produced by fermentation of Microbispora sp. ATCC PTA-5024, the pharmaceutically acceptable salts and compositions thereof, and their use as an antibacterial agent having inhibitory activity versus susceptible microbes. Antibiotic 107891, which is a complex ...

10/13/05 - 20050227916 - Peptide stellate carrier devices for stellate cells
A compound includes a carrier molecule wherein the carrier molecule is linked to a further molecule, wherein the further molecule is at least one cyclic peptide in which the cyclic peptide portion thereof contains at least one sequence encoding a cell receptor recognizing peptide (RRP) and with the proviso that ...

10/13/05 - 20050227915 - Methods and reagents for treating neurodegenerative diseases and motor deficit disorders
The invention relates to a novel method for treating a variety of diseases and disorders, including polyglutamine expansion diseases such as Huntington's disease, neurological degeneration, psychiatric disorders, and protein aggregation disorders and diseases, comprising administering to patients in need thereof a therapeutically effective amount of one or more deacetylase inhibitors. ...

10/13/05 - 20050227914 - New process
The present invention relates to a process for preparing a pharmaceutical starting compound compound by hydrolyzing a compound of the general formula (II): Wherein R1 is protected carboxy, R2 is lower alkoxy or higher alkoxy, A1 is an aromatic bivalent group, heterocyclic bivalent group or cyclo(lower)alkane bivalent group, and A2 ...

10/06/05 - 20050222014 - Multiple agent therapy for sexual dysfunction
Multiple agent therapy for treatment of sexual dysfunction, including male erectile dysfunction, with sequential administration a type V phosphodiesterase inhibitor (PDE-5), such as sildenafil, preferably wherein the PDE-5 inhibitor is administered by oral dose means, and a melanocortin 3 and/or 4 receptor agonist, such as Ac-Nle-cyclo(-Asp-His-D-Phe-Arg-Trp-Lys)-OH (PT-141) preferably wherein the ...

10/06/05 - 20050222013 - Methods for the use of inhibitors of histone deacetylase as synergistic agents in cancer therapy
Improved methods for treatment of cancer are provided. The improvements include the administration of one or more synergistic agents, specifically inhibitors of histone deacetylase proteins and complexes. These synergistic agnets increase the effectiveness of radiation therapy and/or chemotherapies by increasing the sensitivity of tumor cells to treatment. ...

09/15/05 - 20050203006 - Novel lipopeptides as antibacterial agents
The present invention relates to novel lipopeptide compounds. The invention also relates to pharmaceutical compositions of these compounds and methods of using these compounds as antibacterial compounds. The invention also relates to methods of producing these novel lipopeptide compounds and intermediates used in producing these compounds. ...

09/15/05 - 20050203005 - Antibiotic 107891, its factors a1 and a2, pharmaceutically acceptable salts and compositions, and use thereof
The invention relates to an antibiotic substance of microbial origin, arbitrarily denominated antibiotic 107891 which is produced by fermentation of Microbispora sp. ATCC PTA-5024, the pharmaceutically acceptable salts and compositions thereof, and their use as an antibacterial agent having inhibitory activity versus susceptible microbes. Antibiotic 107891, which is a complex ...

09/01/05 - 20050192213 - Echinocandin pharmaceutical formulations containing micelle-forming surfactants
Pharmaceutical formulations are described comprising an echinocandin compound or echinocandin/carbohydrate complex and a pharmaceutically acceptable micelle-forming surfactant in a non-toxic aqueous solvent such that the solubilization of the echinocandin compound is optimized and the ability to freeze-dry the solution is maintained. Both the solution and freeze-dried formulations have increased stability. ...

09/01/05 - 20050192212 - Macrocyclic peptides active against the hepatitis c virus
wherein R1, R2, X, R3, D, and the dotted line b are as defined herein; or a pharmaceutically acceptable salt or ester thereof, are useful as inhibitors of the HCV NS3 protease. ...

08/18/05 - 20050181988 - Echinocandin cyclic peptide derivatives
This invention relates to new lipopeptide compound represented by the following general formula (I) wherein R1, R2, R3, R4 and R5 are as defined in the description or a salt thereof which has antimicrobial activities (especially, antifungal activities), inhibitory activity on β-1,3-glucan synthase, to process for preparation thereof, to a ...

07/28/05 - 20050164922 - Somatostatin agonists
The present invention is directed to cyclic peptides of formula (I): X-A1-cyclo(D-Cys-A3-A4-Lys-A6-A7)-A8-Y, or a pharmaceutically acceptable salt thereof. The peptides bind selectively to the somatostatin subtype receptor type-5 and elicit an agonist effect from the somatostatin subtype receptors. The peptides are useful for treating a variety of diseases, including Cushings ...

07/28/05 - 20050164921 - Depeptidized inhibitors of hepatitis c virus ns3 protease
The present invention discloses novel depeptidized compounds which have HCV protease inhibitory activity as well as pharmaceutical compositions comprising such compounds and methods of using them to treat disorders associated with the HCV protease. ...

07/28/05 - 20050164920 - Compounds that modulate neuronal growth and their uses
Cyclic peptides and peptidomimetics are provided that bind to and/or modulate activities associated with Trk receptors, including processes associated with the growth and repair of the central nervous system (e.g., neuronal growth and survival, axonal growth, neurite outgrowth and synaptic plasticity). Cyclic peptides and peptidomimetics are also provided that block ...

07/21/05 - 20050159347 - Methods for treating hematological disorders through inhibition of dna methylation and histone deacetylase
Methods are provided for treating hematological disorders by inhibition of DNA hypomethylation and histone deacetylase. Such disorders include, for example, acute promyelocytic leukemia, acute lymphoblastic leukemia, chronic myelogenous leukemia, myelodysplastic syndromes, and sickle cell anemia. The methods comprise: administering to a patient suffering from the disease a therapeutically effective amount ...

07/21/05 - 20050159346 - Cyclic peptide antitumor agents
Cyclic peptide compounds and derivatives thereof having antitumor activity as shown by treatment of human melanoma, pancreatic, breast, prostate cancer cells. ...

07/21/05 - 20050159345 - Composition for the treatment of infection by flaviviridae viruses
A is selected from: C1 to C6 alkyl and C3 to C6 cycloalkyl; and B is selected from: phenyl or thiazolyl, both of which optionally substituted with a group selected from NH(R1) and NH(CO)R1, wherein R1 is C1 to C6 alkyl; R is OH or a sulfonamide derivative; or a ...

07/14/05 - 20050153876 - Compositions of lipopeptide antibiotic derivatives and methods of use thereof
The present invention provides derivatives of lipopeptide antibiotics that display antimicrobial activity against microorganisms, methods and compounds for synthesizing such antimicrobial derivatives and analogues, and methods of using the compounds in a variety of contexts, including in the treatment and prevention of microbial infections. ...

06/30/05 - 20050143293 - Peptides for enhancing resistance to microbial infections
The present invention is related to novel bioactive pentapeptides, pentarphins, the main indication of which is enhancing phagocytic activity of macrophages against microbes. In particular, the cyclopentapeptide, cyclo(Val-Lys-Gly-Phe-Tyr), termed cyclopeptarphin, was 100 times more active than tuftsin. Cyclopentarphin was non-toxic even at concentrations 1000 times higher than the minimum active ...

06/23/05 - 20050137128 - Modulators of ß-amyloid peptide aggregation
Compounds that modulate natural β amyloid peptide aggregation are provided. The modulators of the invention comprise a peptide, preferably based on a β amyloid peptide, that is comprised entirely of D-amino acids. Preferably, the peptide comprises 3-5 D-amino acid residues and includes at least two D-amino acid residues independently selected ...

06/09/05 - 20050124536 - Antifungal combination use
There is described antifungal combination use of known antifungal agents such as the azoles or polyenes in combination with a lipopeptide compound antifungal agent. More particularly, the invention relates to antifungal combination use of azoles such as fluconazole, voriconazole, itraconazole, ketoconazole, miconazole, ER 30346 and SCH 56592; polyenes such as ...

06/09/05 - 20050124535 - Cyclic peptide nanotube structures for molecular scale electronic and photonic devices
The stackable cyclic peptide is represented by the general formula of m repeating amino acid residue pairs where n equals 1 or 2, m equals 4 or 6, RA and RD are either H, CH3 or an alkyl, where at least one RB or RE in at least one repeating ...

06/02/05 - 20050119168 - Macrocyclic inhibitors of hepatitis c virus ns3-serine protease
wherein Z′, L′, M′, R1, X and D are defined herein. ...

06/02/05 - 20050119167 - Process for the preparation of cyclic peptides
The present invention relates to a process for the preparation of cyclic peptides, in particular the preparation of Ac-Phe[Orn-Pro-D-Cha-Trp-Arg] known as 3D53 or PMX53 which is a macrocyclic peptidomimetic of the human plasma protein C5a and displays excellent anti-inflammatory activity. ...



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