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Drug, Bio-affecting And Body Treating Compositions > Designated Organic Active Ingredient Containing (doai) > Heterocyclic Carbon Compounds Containing A Hetero Ring Having Chalcogen (i.e., O,s,se Or Te) Or Nitrogen As The Only Ring Hetero Atoms Doai > Hetero Ring Is Six-membered Consisting Of Two Nitrogens And Four Carbon Atoms (e.g., Pyridazines, Etc.) > 1,4-diazine As One Of The Cyclos > Pyrimidines With Chalcogen Bonded Directly To A Ring Carbon Of Said Pyrimidine Moiety

Pyrimidines With Chalcogen Bonded Directly To A Ring Carbon Of Said Pyrimidine Moiety

Pyrimidines With Chalcogen Bonded Directly To A Ring Carbon Of Said Pyrimidine Moiety 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.

02/01/07 - 20070027172 - Crystalline pharmaceutical
New crystalline forms of lopinavir are disclosed. ...

01/25/07 - 20070021451 - Method for preventing or treating neurologic damage after spinal cord injury
or a salt, or a solvate thereof, and a use thereof. ...

01/25/07 - 20070021450 - Indanylamino uracils and their use as antioxidants and neuroprotectants
enantiomers, tautomers, and pharmaceutically acceptable salts of the compounds, pharmaceutical compositions containing such compounds or salts, and processes for their preparation. The subject invention also provides methods of alleviating symptoms of neurologic and inflammatory disorders, methods of preventing oxidation of lipids, proteins, or deoxyribonucleic acids on a cellular level, and ...

01/25/07 - 20070021449 - Pyrimidine derivatives for the prevention of hiv infection
This invention concerns the use of a compound for the manufacture of a medicament for the prevention of HIV infection via sexual intercourse and related intimate contact between partners, wherein the compound is a compound of formula (I) a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a ...

01/18/07 - 20070015778 - Gonadotropin-releasing hormone receptor antagonists and methods relating thereto
wherein R1a, R1b, R2a, R2b, R3, R4, R5, R6, R7 and X are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof ...

12/28/06 - 20060293353 - Matrix metalloproteinase inhibitors
R14 and R15 each independently represent H, C1-6 alkyl, C1-4 alkylaryl or C1-4 alkylheteroaryl or together with the functionality to which they are attached R14 and R15 form a heterocyclic or fused heterocyclic group; and physiologically functional derivatives thereof, corresponding processes for preparation, pharmaceutical formulations containing them and their use ...

12/28/06 - 20060293352 - Phenoxiacetic acid derivatives
The invention relates to certain 2-substituted phenoxyacetic acid derivatives of formula (I), in which the variables are as defined in the claims, useful in the treatment of diseases or conditions in which modulation of the CRTh2 receptor is beneficial, such as asthma and rhinitis. ...

12/21/06 - 20060287346 - Pharmaceutical formulation comprising a pyrimidine-a-one derivative coated with an enteric polymer
The present invention provides enteric polymer coated tablet formulations for oral administration which comprise a phospholipase A2 enzyme Lipoprotein Associated Phospholipase A2 (Lp-PLA2) inhibitor, processes for preparing such formulations and their use in therapy, in particular the treatment of atherosclerosis. ...

12/21/06 - 20060287345 - Substituted 4-phenyl-4-[1h-imidazol-2-yl]-piperidine derivatives as selective non-peptide delta opiod agonists with antidepressant and anxiolytic activity
The present invention relates to the use of 4-phenyl-4-[1H-imidazol-2-yl]-piperidine derivatives according to Formula (I) the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the tautomeric forms thereof and the N-oxide forms thereof as selective non-peptide δ-opioid agonists for use in the prevention and/or treatment of ...

12/07/06 - 20060276494 - Novel sulfonamides as l-cpt1 inhibitors
wherein R2, R3, R4, A, X, Y1, Y2, Y3, Y4 and Z1 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit L-CPT1 and can be used as medicaments. ...

12/07/06 - 20060276493 - Alpha- and beta-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors
α- and β-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as-inhibitors of HIV protease. ...

12/07/06 - 20060276492 - Antiviral activity and resolution of 2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane
A method and composition for the treatment of HIV and HBV infections in humans is disclosed that includes administering an effective amount of 2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane, a pharmaceutically acceptable derivative thereof, including a 5′ or N4 alkylated or acylated derivative, or a pharmaceutically acceptable salt thereof, in a pharmaceutically acceptable carrier. A ...

11/30/06 - 20060270693 - Ether derivative
wherein each symbol is as defined in the description; a pharmaceutical composition containing the ether derivative; and a package containing the pharmaceutical composition and a description of use thereof. A pharmaceutical composition of the present invention, which contains this compound of the present invention has a superior anti-inflammatory and analgesic ...

11/16/06 - 20060258694 - Histone deacetylase inhibitors
wherein the variables are as defined herein. ...

11/09/06 - 20060252785 - Heterocyclic antiviral compounds
Compounds having the formula I wherein A, m and R1 are herein defined are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for inhibiting hepatitis replication, processes for making the compounds and synthetic intermediates used in the process ...

11/02/06 - 20060247260 - Bis (hetero) aryl carboxamide derivatives for use as pg12 antagonists
in which Ar1 and Ar2 independently represent phenyl or a 5 or 6-membered heteroaromatic ring, R6 represents carboxyl or tetrazolyl, and the remaining variables are as defined in the text and claims, which are useful as an active ingredient of pharmaceutical preparations. The aryl or heteroaryl amido alkanes of the ...

10/19/06 - 20060235035 - Novel methoxybenzamibe compounds for use in mch receptor related disorders
Novel compounds of Formula (I) which modulate MCH activity are disclosed, in which A is a linker; Ar1 is an aryl or heteroaryl group; R1 is a lower alkoxy group; R2 is an R1 group or hydrogen, an OH or an NH2 group, Q together with the carbonyl forms an ...

10/12/06 - 20060229326 - Pyridine-3-carboxamide derivatives as cb1 inverse agonists
wherein X and R1 to R8 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with the modulation of CB1 receptors, such as obesity. ...

10/12/06 - 20060229325 - N-aryl-sulfoximine-substituted pyrimidines as cdk-and/or vegf inhibitors, their production and use as pharmaceutical agents
in which Q, R1, R2, R3, R4, R5, X, and m have the meanings that are contained in the description, as inhibitors of cyclin-dependent kinases and VEGF-receptor tyrosine kinases, their production as well as their use as medications for treatment of various diseases. ...

09/28/06 - 20060217403 - Substituted 2-aminoacetamides and the use thereof
and to pharmaceutically acceptable salts and prodrugs thereof, wherein the substituents are defined herein. The invention is also directed to the use of substituted 2-aminoacetamides in methods for the treatment of neuronal damage following global and focal ischemia, and for the treatment, prevention or amelioration of pain, as anticonvulsants, as ...

09/28/06 - 20060217402 - Biocidal compounds and their preparation
wherein R is H or CH3. Of particular interest are two isomers that are named malayamycin A and desmethylmalayamycin A. These isomers, which may be prepared by growing under controlled conditions a previously unknown strain of micro-organism from the species Streptomyces malaysiensis, are characterised by nmr and mass spectroscopic data. ...

09/21/06 - 20060211720 - Heterocyclic compounds as inhibitors of factor viia
The present invention relates generally to compounds that inhibit serine proteases. In particular it is directed to novel heterocyclic compounds, or a stereoisomer or pharmaceutically acceptable salt, solvate, or prodrug form thereof, which are useful as selective inhibitors of serine protease enzymes of the coagulation cascade; for example thrombin, factor ...

09/21/06 - 20060211719 - Heteroaryl aminoguanidine and alkoxyguanidines and their use as protease inhibitors
wherein X is O or NR9 and Het, R1, R7, R8, R12-R15, Ra, Rb, Rc, Z, and n are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin. Also described are methods for preparing such compounds. The ...

08/31/06 - 20060194824 - Compositions containing pyrimidine derivatives as inhibitors of cox-2
in which the compound is present in solid particles in nanoparticulate form in admixture with one or more pharmaceutically acceptable carriers or excipients. ...

08/24/06 - 20060189640 - Method of increasing drug oral bioavailability and compositions of less toxic orotate salts
The present invention relates generally to the method of increasing the oral bioavailability, reducing chemotherapy induced toxicity and side effects, and improving the effectiveness of pharmaceutical agents that are poorly absorbed from the gastrointestinal tract. Specifically, the invention relates to poorly absorbed pharmaceutical drugs and converting them to orotate salts. ...

08/10/06 - 20060178387 - Combined treatment with capecitabine and an epidermal growth factor receptor kinase inhibitor
The present invention provides a method for treating tumors or tumor metastases in a patient, comprising administering to the patient simultaneously or sequentially a therapeutically effective amount of an EGFR kinase inhibitor and capecitabine combination, with or without additional agents or treatments, such as other anti-cancer drugs or radiation therapy. ...

07/27/06 - 20060167031 - Method of administrating an anticancer drug containing alpha, alpha, alpha-trifluorothymidine and thymidine phosphorylase inhibitor
The present invention relates to a method for treating a cancer comprising orally administering a composition containing α,α,α-trifluorothymidine (FTD) and 5-chloro-6-(1-(2-iminopyrrolidinyl)methyl)uracil hydrochloride in a molar ratio of 1:0.5 at a dose of 20 to 80 mg/m2/day in terms of FTD in 2 to 4 divided portions per to patients in ...

07/20/06 - 20060160833 - Plant protection agents
The present invention relates to a microbicide composition for plants, containing at least two active ingredient components in an amount producing synergistic activity, together with an appropriate filler, wherein component I is the compound 2-[α-{[(α-methyl-3-trifluoromethyl-benzyl)imino]-oxy}-o-tolyl]-glyoxylic acid-methylester-O-methyloxime, and component II is a compound selected from the group consisting of IIA) 5,7-dichloro-4-(4-fluorophenoxy)quinoline ...

07/06/06 - 20060148834 - Novel coumarin-amide derivatives and its preparation, said drug composition and its use
The present invention relates to novel coumarin derivatives, their carboxamides, pharmaceutical compositions containing them and their uses as drugs for kidney protection, treating drugs of hypertension, cardio-cerebrovascular diseases, non-insulin dependent diabetes, tumor, pre-cancerous lesion, and edemas. ...

07/06/06 - 20060148833 - Use of chymase inhibitors for the prevention and/or treatment of arterio-venous graft failure
Disclosed is a method of treating A-V graft failure in a subject in need of such treatment, said method comprising administering to said subject an effective amount of an agent that inhibits the production, release or neo-intima generating effects of chymase, wherein said effective amount of said agent is an ...

06/29/06 - 20060142318 - Compounds for treating fundic disaccomodation
wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ═NR9; Y2 is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or ...

06/15/06 - 20060128733 - Method for treating hiv infection through co-administration of tipranavir and reverset
A method for treating HIV infection through co-administration of tipranavir and reverset. ...

06/08/06 - 20060122207 - Imidazol derivatives as raf kinase inhibitors
one of X1 and X2 is N and the other is NR6, wherein R6 is hydrogen, C1-6alkyl, or arylC1-6alkyl or pharmaceutically acceptable salts thereof, their use as inhibitors of Raf kinases, and pharmaceutical compositions containing them. ...

06/08/06 - 20060122206 - Tetrahydropyridin-4-yl indoles with a combination of affinity for dopamine-d2 receptors and serotonin reuptake sites
A and Z together form a saturated or (partly) unsaturated 5- or 6-membered ring which may be substituted with halogen, alkyl (C1-3) or phenyl, in which ring Z represents carbon, sulfur of nitrogen. ...

06/08/06 - 20060122205 - Potassium salt of an hiv integrase inhibitor
Compound A is an HIV integrase inhibitor useful for treating or prophylaxis of HIV infection, for delaying the onset of AIDS, and for treating or prophylaxis of AIDS. ...

06/08/06 - 20060122204 - Gonadotropin-releasing hormone receptor antagonists and methods relating thereto
wherein n, R1a, R1b, R1c, R2a, R2b, R3, R4, R5, R6 and X are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use ...

06/08/06 - 20060122203 - 2-hydroxymethylcyclopropylidenemethylpurines and - pyrimidines as antiviral agents
wherein B is a purine or pyrimidine heterocyclic ring and is preferably selected from the group consisting of 6-aminopurine (adenine), 2,6-diaminopurine, 2-amino-6-azidopurine, 2-amino-6-cyclopropylaminopurine, 6-hydroxypurine (hypoxanthine), 2-amino-6-halo substituted purines, 2-amino-6-alkoxy substituted purines, 2-amino-6-hydroxypurine (guanine), 3-deazapurines, 7-deaza-purines, 8-azapurines, cytosine, 5-halo substituted cytosines, 5-alkyl substituted cytosines, thymine, uracil and 6-azapyrimidines; X is O; ...

06/08/06 - 20060122202 - Gonadotropin-releasing hormone receptor antagonists and methods relating thereto
wherein R1a, R1b, R1c, R2a, R2b, R3, R4, R5, R6 and X are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof ...

06/08/06 - 20060122201 - Uracil-thioether
The invention relates to uracil-thioethers, pharmaceutical compositions containing said compounds and to a method for the production thereof. The invention also relates to the use of said substances in the treatment of diseases in humans and animals. ...

06/01/06 - 20060116390 - Hepatitis c virus inhibitors
The present invention relates to new compounds useful for the treatment or prevention of hepatitis C, process for preparing them, and a composition for the treatment or prevention of hepatitis C comprising the compounds as an active ingredient. ...

06/01/06 - 20060116389 - Antibacterial oxazolidinones
A compound of the formula (I), or a pharmaceutically-acceptable salt, or in-vivo hydrolysable ester thereof: formula (I) wherein C is selected from D and E, formula (II) R2a, R6a, and R3a are independently selected from for example H, CF3, Me and Et; R2b and R6b are independently selected from for ...

05/25/06 - 20060111378 - Substituted 2-anilinopyrimidines as cell-cycle-kinase or receptor-tyrosine-kinase inhibitors, their production and use as pharmaceutical agents
in which R1, R2, R3, R4, A and D have the meanings that are contained in the description, as inhibitors of cyclin-dependent kinases and VEGF receptor tyrosine kinases, their production as well as their use as medications for treating various diseases. ...

05/25/06 - 20060111377 - Heterocyclic derivatives
The invention relates to novel heterocyclic derivatives, processes for their preparation, and their use in medicaments, especially for the treatment of chronic obstructive pulmonary diseases, acute coronary syndrome, acute myocardial infarction and heart failure development. ...

05/18/06 - 20060106044 - Methods for inhibiting the transmission of hiv using topically applied substituted 6-benzyl-4-oxopyrimidines
A method for inhibiting sexual transmission of HIV comprising topically applying to the skin or epithelial tissue of a human a composition comprising a non-nucleoside reverse transcriptase inhibitor (“NNRTI”) that is able to inhibit viral replication for periods exceeding 12, 24, or even 36 days, at concentrations below even 10 ...

05/18/06 - 20060106043 - Method for treating hiv infection through co-administration of tipranavir and etravirine
A method for treating HIV infection through co-administration of tipranavir and etravirine. ...

05/18/06 - 20060106042 - Substituted heterocyclpyrmidines
in which n is 0, 1, or 2, R is hydrogen of fluorine, and X, Y, and Z are as defined in the disclosure, to a method for their production, and to their use as pesticides. ...

05/11/06 - 20060100226 - 2-thiopyrimidinones as therapeutic agents
The present invention provides compounds of Formulas I-VII, or pharmaceutically acceptable derivatives thereof, wherein the compounds are as defined in the specification. These compounds are inhibitors of protein kinases, particularly inhibitors of MEKK protein kinases. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods ...

05/11/06 - 20060100225 - Heteroaryl guanidines; inhibitors of viral replication
Certain compounds of Formula 1 described herein which possess potent antiviral activity. Certain compounds of Formula 1 that are potent and/or selective inhibitors of Hepatitis C virus replication. Pharmaceutical compositions containing one or more compounds of Formula 1, or a salt, solvate, or acylated prodrug of such compounds, and one ...

05/11/06 - 20060100224 - Piperidine ouracil used as a medicament for treating bacterial infections
The invention relates to piperidine ouracil and a method for the production thereof in addition to the use thereof in the production of medicaments for treating and/or in the prophylaxis of diseases, especially bacterial diseases. ...

05/04/06 - 20060094737 - Novel uracil derivatives and medicinal use thereof
It is intended to provide an uracil derivative represented by the following general formula (I): (I) wherein X represents a group selected from among NHCO, NHCH2, CO, CONH and CH2NH; R1 represents hydrogen or optionally substituted C1-6 alkyl; R2 represents a group of the following general formula (II) or (III): ...

04/13/06 - 20060079542 - Compounds and methods for treating insulin resistance and cardiomyopathy
Novel compounds, compositions comprising compounds, and methods for methods for preparing and using compounds are described herein. Methods of treating or ameliorating various conditions, including insulin resistance, pancreatic beta cell apoptosis, obesity, pro-thrombotic conditions, myocardial infarction, hypertension, dyslipidemia, manifestations of Syndrome X, congestive heart failure, inflammatory disease of the cardiovascular ...

03/30/06 - 20060069109 - Therapeutic agents
A compound of the Formula: (I) (A chemical formula should be inserted here—please see paper copy enclosed herewith) Formula: (I); for use as a Tie2 receptor tyrosine kinase inhibitor in a warm-blooded animal such as man. ...

03/23/06 - 20060063789 - Aminobenzamide derivatives as glycogen synthase kinase 3 beta inhibitors
a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein ring A represents a 6-membered heterocycle; R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; optionally substituted C1-6alkyl; C1-6alkyloxycarbonyl; optionally substituted C1-6alkyloxyC1-6alkylcarbonyl; X is a direct bond or a linker atom or group; Z is O ...

03/16/06 - 20060058326 - Pyrimidines, methods for the production thereof, and use thereof
R3 is a five- or six-membered saturated, partially unsaturated or aromatic mono- or bicyclic heterocycle which contains one to four heteroatoms from the group consisting of O, N and S; and processes and intermediates for preparing these compounds, compositions comprising them and their use for controlling phytopathogenic harmful fungi are ...

03/09/06 - 20060052405 - Hair loss prevention
Compositions to prevent or reduce hair loss, allowing the body to maintain normal, healthy hair growth, comprising a penetration enhancer together with a testosterone blocker or a vascular enhancer, or both. ...

02/23/06 - 20060040967 - Pyrimidine derivative as selelctive cox-2 inhibitors
or a pharmaceutically acceptable salt thereof. Compounds of formula (I) are potent and selective inhibitors of COX-2 and are of use in the treatment of the pain, fever and inflammation of a variety of conditions and diseases. ...

02/16/06 - 20060035914 - Compositions and methods for the treatment of disorders of the central and peripheral nervous systems
The present invention relates to methods and compositions for treating selected conditions of the central and peripheral nervous systems employing non-synaptic mechanisms. More specifically, one aspect of the present invention relates to methods and materials for treating seizure and seizure disorders, epilepsy, status epilepticus, migraine, spreading depression, intracranial hypertension; for ...

02/16/06 - 20060035913 - Method for the production of 2-amino-4-chloro-6-alkoxypyrimidines
The present invention provides a process for preparing 2-amino-4-chloro-6-alkoxypyrimidines by reacting the 2-amino-4,6-dichloropyrimidine with an alkali metal alkoxide or a mixture of alkali metal hydroxides and an alcohol, in which the reaction is effected in a polar aprotic solvent (or solvent mixture), the solvent is subsequently distilled off to an ...

02/02/06 - 20060025433 - Pyrimidine derivatives useful as inhibitors of pkc-theta
wherein X, Y, R1, R2 and R3 are as defined herein, which are useful as inhibitors of PKC-theta and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC-theta, including immunological disorders and type II diabetes. This invention also ...

02/02/06 - 20060025432 - Pyrimidyl sulphone amide derivatives as chemokine receptor modulators
A compound of formula (I), pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof for the treatment of asthma, allergic rhinitis, COPD, inflammatory bowel disease, irritable bowel syndrome, osteoarthritis, osteoporosis, rheumatoid arthritis, psoriasis or cancer. ...

01/19/06 - 20060014768 - Pyrimidine compound and medical use thereof
wherein each symbol is as defined in the specification and a method of therapeutically or prophylactically treating an undesirable cell proliferation, comprising administering such a compound. The compound of the present invention has superior activity in suppressing undesirable cell proliferation, particularly, an antitumor activity, and is useful as an antitumor ...

01/19/06 - 20060014767 - Heterocyclic antiviral compounds
Chemokine receptor antagonists, in particular, 3,7-diazabicyclo[3.3.0]octane compounds according to formula (I) are antagonists of chemokine CCR5 receptors which are useful for treating or preventing an human immunodeficiency virus (HIV) infection, or treating AIDS or ARC. The invention further provides methods for treating diseases that are allieviated with CCR5 antagonists. The ...

01/19/06 - 20060014766 - Crystalline salts of 7- '4-(4-fluorophenyl) -6-isopropyl-2-'methyl (methylsulfonyl) amino! pyrimidin-5-yl!- (3r, 5s) - 3, 5-dihydroxyhept-6-enoic acid
The invention relates to crystalline salts of the compound (E)-7-[4-(4-fluorophenyl)isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl]-(3R,5S)-3,5-dihydroxyhept-6-enoic acid of formula (I), as well as processes for their manufacture, pharmaceutical compositions containing them, and their uses. ...

01/05/06 - 20060004030 - Pyrimidine derivatives as modulators of chemokine receptor activity
Compounds of formula (1), pharmaceutically acceptable salts, solvates and in vivo hydrolysable esters thereof, have activity as pharmaceuticals, in particular as modulators of chemokine receptor (especially CXCR2) activity, and may be in the treatment (therapeutic or prophylactic) of conditions/diseases in human and non-human animals which are exacerbated or caused by ...

01/05/06 - 20060004029 - Nitrogen-containing aromatic derivatives
wherein X1 represents a nitrogen atom or a group represented by the formula —CR10═; X2 represents a nitrogen atom or a group represented by the formula —CR11═; Y represents an oxygen atom or the like; R1 represents a C1-6 alkoxy group, an optionally substituted C6-10 aryloxy group, a group represented ...

12/29/05 - 20050288315 - Dual molecules containing a peroxide derivative, synthesis and therapeutic applications thereof
Rx or Ry is a cyclic peroxide with 4 to 8 chain links, which may comprise 1 or 2 additional oxygen atoms in the cyclic structure, and one or more substituents R3, identical or different, at least one representing a halogen atom, an —OH group, a —CF3 group, an aryl, ...

12/22/05 - 20050282841 - Novel esters as useful broad spectrum fungicidal compounds
The instant invention relates to the discovery of certain novel fungicidal esters of agriculturally active acids. These esters can present agronomical advantages over traditional fungicidal products by presenting multiple fungicidal mechanisms that ensure activity over a broad fungi spectrum while limiting the appearance of fungi resistance. ...

12/22/05 - 20050282840 - Methods of modulating neurotrophin-mediated activity
Disclosed are compositions which modulate the interaction of nerve growth factor and brain-derived neurotrophic factor with neurotrophic receptors. Also disclosed are methods of using the compositions of the invention, including methods of administration. ...

12/22/05 - 20050282839 - Pyrimidyl phosphonate antiviral compounds and methods of use
Pyrimidine I and pyrimidinone II phosphonate compounds and methods for viral inhibition are disclosed. The compounds include at least one phosphonate group covalently attached at any site. ...

12/22/05 - 20050282838 - Compounds, compositions, and methods
Compounds useful for treating cellular proliferative diseases are disclosed. ...

12/22/05 - 20050282837 - 5-substituted pyrimidine derivatives of conformationally locked nucleoside analogues
The embodiments described herein concern 5-substituted pyrimidine derivatives of conformationally locked nucleoside analogues and to the use of these derivatives as anti-viral and anti-cancer agents. ...

12/01/05 - 20050267140 - Method for treating abnormal cell growth
Therapeutic pharmaceutical compositions and methods of treatment of abnormal cell growth comprising a pyrimidine derivative or a pharmaceutically acceptable salt, solvate or prodrug thereof in combination with an oral camptothecin, an oral camptothecin derivative, an indolopyrrocarbazole derivative or a pharmaceutically acceptable salt, solvate or prodrug thereof for the treatment of ...

11/24/05 - 20050261323 - Medical uses of novel carbamate-substituted pyrazolopyridine derivatives
wherein R1 is H or a di-C1-6-alkylaminocarbonyl radical, and R2 is a radical of the formula —O—C(X)—NR3R4 wherein X is O or S. The compound may also be administered in combination with at least one organic nitrate or NO donor, or in combination with at least one compound which inhibits ...

11/24/05 - 20050261322 - Hiv integrase inhibitors
Compounds of the present disclosure are spirocycle-substituted pyrimidinecarboxamides. Also disclosed are pharmaceutical compositions comprising the compounds, and methods of using the compounds. The compounds are useful for treating HIV infection and AIDS. ...

11/24/05 - 20050261321 - Substituted organosulfur compounds and methods of using thereof
The present invention provides substituted di-, tri-, tetra- and penta-sulfide compounds and compositions, and methods of using the same for the treatment and/or prevention of a cell proliferative disorder. The present invention also provides methods for preparing trisulfide compounds and compositions. ...

11/24/05 - 20050261320 - Compounds and methods for the treatment of cancer
(−)-(2S,4S)-1-(2-Hydroxymethyl-1,3-dioxolan-4-yl)cytosine (also referred to as (−)-OddC) or its derivative and its use to treat cancer in animals, including humans. ...

11/03/05 - 20050245553 - Methods of treating medical conditions using sulfonate-substituted pyrazolopyridine derivatives
wherein R1 is a radical of the formula —O—SO2-R3 in which R3 is optionally substituted C1-6-alkyl, optionally substituted C3-8-cycloalkyl, or optionally substituted phenyl; R2 is H, optionally substituted C1-6-alkyl-CO— or optionally substituted C1-6-alkyl-SO2—; as well as salts, stereoisomers, tautomers, and hydrates thereof. ...

11/03/05 - 20050245552 - N-substituted pyridinone and pyrimidinone derivatives for use as lp-pla2 inhibitors in the treatment of artherosclerosis
are inhibitors of the enzyme Lp-PLA2 and are of use in therapy, in particular for treating atherosclerosis. In Formula I R1, R2, R3, R4, R5, R6, X and Y. ...

10/20/05 - 20050234082 - Gonadotropin-releasing hormone receptor antagonists and methods relating thereto
wherein A, Q, R1, R2, R3a, R3b, R4, R5, R6 and n are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof ...

10/20/05 - 20050234081 - Novel thiophene amidines, compositions thereof, and methods of treating complement-mediated diseases and conditions
Disclosed is a method for treating the symptoms of an acute or chronic disorder mediated by the classical pathway of the complement cascade, comprising administering to a mammal in need of such treatment a therapeutically effective amount of a compound of Formula (I) or a solvate, hydrate or pharmaceutically acceptable ...

10/20/05 - 20050234080 - Mitotic kinesin inhibitors
The present invention relates to dihydropyrimidone compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals. ...

10/13/05 - 20050228004 - Imidazo'1,2-a!pyridine derivatives for the prophylaxis and treatment of herpes viral infections
wherein all variables are as defined herein, pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceutical agents. ...

10/06/05 - 20050222185 - Nucleoside derivatives and therapeutic uses therof
The present invention relates to nucleoside derivatives represented by general formulas I and II, their synthetic methods and their pharmacologically acceptable salts thereof, and compositions containing such compounds. Methods for treating hyperproliferative disorders by administering the compounds are also included. ...

10/06/05 - 20050222184 - Process for preparing (s)-tetrahydro-a-(1-methylethyl)-2-oxo-1(2h)-pyrimidineacetic acid
A process for preparing (S)-tetrahydro-a-(1-methylethyl)-2-oxo-1(2H)-pyrimidineacetic acid, an intermediate that is useful in the synthesis of HIV protease inhibitors such as, for example, those described in U.S. Pat. No. 5,914,332, is described. The process under consideration comprises the following steps:—L-valine is reacted with acrylonitrile;—the N-(2-cyanoethyl)-L-valine thus obtained is isolated and then ...

09/29/05 - 20050215578 - Thiadiazole compounds and use thereof
R2 represents phenyl C1-C4 alkyl in which phenyl may be substituted, pyridyl C1-C4 alkyl in which pyridyl may be substituted, or pyrimidyl C1-C4 alkyl in which pyrimidyl may be substituted; has an excellent arthropod pests controlling activity. ...

09/22/05 - 20050209257 - 5-protected aminopyrimidine compound, production method thereof and intermediate therefor
The present invention provides a production method of 5-aminopyrimidine compound represented by the formula (5) by reacting a glycine compound represented by the formula (1) with t-butoxybisdimethylaminomethane, dimethylformamidedimethylacetal or dimethylformamidediethylacetal to produce a dialkylaminomethylene compound represented by the formula (2), reacting the compound of formula (2) in the presence of ...

09/15/05 - 20050203114 - Kinase inhibitors
The invention relates to inhibitors of kinases, compositions comprising the inhibitors, and methods of using the inhibitors and inhibitor compositions. The inhibitors and compositions comprising them are useful for treating disease or disease symptoms. The invention also provides for methods of making kinase inhibitor compounds, methods of inhibiting kinase activity, ...

09/15/05 - 20050203113 - Compounds and method for the treatment of overactive bladder
wherein in said compounds D, A, R1, R3 and R4 are as defined in the specification. Pharmaceutically-advantageous salts of the compounds, methods of use of the compounds, either alone or in combination with other pharmacological agents, and pharmaceutical compositions useful in practicing the methods of the invention are also disclosed. ...

09/01/05 - 20050192301 - Stereoisomers and stereoisomeric mixtures of 1-(2,4-pyrimidinediamino)-2-cyclopentanecarboxamide synthetic intermediates
The present invention provides stereoisomers and stereoisomeric mixtures of 1-(2,4-pyrimidinediamino), 2-formamido cyclopentyl intermediates useful for the preparation of compounds having antiproliferative activity and methods to prepare the intermediates. ...

09/01/05 - 20050192300 - Pyrimidine compounds
The present invention relates to substituted pyrimidines of formula I, their preparation, pharmaceutical compositions containing them and their use as inhibitors of cyclin-dependent kinases (CDKs) and hence their use in the treatment of proliferative disorders and/or viral disorders. ...

09/01/05 - 20050192299 - Method of treating or preventing hepatitis b virus
Anti-hepatitis B virus compounds (−)3′-thia-2′,3′-dideoxycytidine, (−)5-fluoro-3′-thia-2′,3′-dideoxycytidine, (±) β-dioxolane cytosine and (−)-L-B-dioxolane cytosine. A method of treating a patient suffering from hepatitis B virus or preventing hepatitis B virus infection comprising administering to the patient an effective amount of an active compound selected from the group consisting of (a) (−)3′-thia-2′,3′-dideoxycytidine, (b) ...

08/25/05 - 20050187235 - Pyrimidine derivatives useful as selective cox-2 inhibitors
Methods of treating a subject suffering from a condition which is mediated by COX-2. ...

08/11/05 - 20050176744 - Novel heteroaryl derivatives and their use as medicaments
The invention relates to novel quinoline derivatives of the formula 1, to their preparation and to their use as medicaments, in particular for treating tumors. ...

08/11/05 - 20050176743 - Sulfoximine-substituted pyrimidines as cdk-and/or vegf inhibitors, their production and use as pharmaceutical agents
in which Q, R1, R2, R3, R4, R5, X, and m have the meanings that are contained in the description, as inhibitors of cyclin-dependent kinases and VEGF-receptor tyrosine kinases, their production as well as their use as medications for treatment of various diseases. ...

08/04/05 - 20050171130 - Pyrimidine compounds and their use as pesticides
wherein R1 is C3-C7 alkynyl; R2 is hydrogen, halogen, or C1-C3 alkyl; and R3 is C1-C8 alkyl that may be substituted with halogen or C1-C3 alkoxy, or C3-C6 cycloalkyl (that may be substituted with halogen or C1-C3 alkyl) C1-C3 alkyl; a pesticidal composition comprising the pyrimidine compound as an active ...

07/14/05 - 20050153995 - Nonnucleoside inhibitors of reverse transcriptase, composite binding pocket and methods for use thereof
Novel compounds that are potent inhibitors of HIV reverse transcriptase (RT) are described in the invention. Thes novel compounds also inhibit replication of a retrovirus, such as human immunodeficiency virus-1 (HIV-1). The novel compounds of the invention include analogs and derivatives of phenethylthiazolylthiourea (PETT), of dihydroalkoxybenzyloxopyrimidine (DABO), and of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine ...

07/14/05 - 20050153994 - The use of 5-fluorourcil, delivered by iontophoresis as an inhibitor of cell proliferation in the eye, bulbar and palpebral conjunctiva, eyelid, peri-orbital soft tissues and skin
A method for treating neoplastic, angiogenic, fibroblastic, and/or immunosuppressive ocular irregularities of a living subject, comprising the steps of: providing a living subject, wherein the living subject includes an affected ocular area having a neoplastic, angiogenic, fibroblastic, and/or immunosuppressive irregularity; providing a 5′ fluorouracil based medicament, wherein the 5′ fluorouracil ...

07/14/05 - 20050153993 - Treatment of statin side effects using uridine derivatives
The invention relates generally to treatment of muscle pain and/or fatigue and to methods of treatment of side effects of statin therapy which involve the administration of uridine, biological precursors or derivatives or uridine or salts, esters, tautomers or analogues thereof, which are collectively referred to as uridine related compounds. ...

07/07/05 - 20050148612 - Reversing, postponing or preventing the occurrence of gtn tolerance and/or generation of reactive oxygen species from mitochondria
A patient in need of nitroglycerin therapy is treated with nitroglycerin and agent that prevents inhibition of or reverses inhibition of mtALDH and/or the generation of reactive oxygen species from mitochondria, e.g., a mitochondrial antioxidant which is not a reducing agent or a dithiol, e.g., ebselen or uric acid. Nitroglycerin ...

07/07/05 - 20050148611 - Compounds capable of activating cholinergic receptors
The present invention generally relates to nicotinic compounds, in the form of aryl substituted olefinic compounds, as well as pro-drug, N-oxide, metabolite and pharmaceutically acceptable salt forms thereof. Methods of modulating neurotransmitter release via administration of the compounds, pro-drugs, N-oxides and/or pharmaceutically acceptable salts are also disclosed. ...

07/07/05 - 20050148610 - 6,7-dihydro-5h-pyrazolo[1,2-a]pyrazol-1-ones which control inflammatory cytokines
The present invention relates to methods for treating diseases or disease states which are mediated or otherwise affected by the extracellular release of cytokines, said method comprising the step of administering to a human or higher mammal in need of treatment, one or more of the 6,7-dihydro-5H-pyrazolo[1,2a]pyrazol-1-ones of the present ...

06/30/05 - 20050143404 - Solid pharmaceutical dosage formulation
The present invention provides a pharmaceutical dosage formulation, and more particularly, to a pharmaceutical dosage formulation comprising an HIV protease inhibitor. ...

06/30/05 - 20050143403 - Substituted pyrimidinones and pyrimidinthiones
This invention relates to substituted pyrimidinone and pyrimidithione derivatives that bind with high affifnity to CRF1 receptors, including human CRF1 receptors. This invention also relates to methods of using the compounds of the invention to treat a disorder or condition, the treatment of which can be effected or facilitated by ...

06/23/05 - 20050137216 - Heterocyclic sodium/proton exchange inhibitors and method
wherein n is 1 to 5; X is N or C—R5 wherein R5 is H, halo, alkenyl, alkynyl, alkoxy, alkyl, aryl or heteroaryl; Z is a heteroaryl gorup, R1, R2, R3 and R4 are as defined herein, and where X is N, R1 is preferably aryl or heteroaryl, and are ...

06/16/05 - 20050130998 - 2-amino-3-(alkyl)-pyrimidone derivatives
R4 represents a C1-10 alkyl group optionally substituted by a hydroxyl group, amino, C1-6 monoalkylamino group, C2-12 dialkylamino group or C6,10 aryl group which may be substituted. And a medicament comprising the said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment ...

06/16/05 - 20050130997 - Pyrimidinone viral polymerase inhibitors
A class of pyrimidinone derivatives of formula (I): wherein Z, R1, R2 and R3 are as defined herein; and pharmaceutically acceptable salts thereof; are inhibitors of viral polymerases, especially (the hepatitis C virus (HCV) polymerase enzyme. ...

06/09/05 - 20050124639 - Process for the preparation of pyrimidine derivatives
wherein R4 is hydrogen, a lower alkyl or a cation capable of forming a non-toxic pharmaceutically acceptable salt and each R5 are the same or different and are hydrogen or a hydrolyzable protecting group, or each R5, together with the oxygen atom to which each is bonded, form a hydrolyzable ...



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