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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 > Nitrogen Bonded Directly To The 1,3-diazine At 2-position By A Single Bond Nitrogen Bonded Directly To The 1,3-diazine At 2-position By A Single BondNitrogen Bonded Directly To The 1,3-diazine At 2-position By A Single Bond 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.01/25/07 - 20070021452 - Pyrimidin-4-yl-3, 4-thione compounds and their use in therapy Further aspects of the invention relate to pharmaceutical compositions comprising such compounds, and their use in the preparation of a medicament for treating one or more of the following: a proliferative disorder, a viral disorder, a CNS disorder, a stroke, alopecia and diabetes. ... 01/18/07 - 20070015779 - Compositions and treatments for inhibiting kinase and/or hmg-coa reductase The present invention provides compositions of matter; kits and methods for their use in the treatment of MAP kinase-related conditions and/or HMG-CoA reductase-related conditions. In particular, the invention provides compositions for treating inflammatory and/or cardiovascular conditions in an animal subject by inhibiting p38α MAP kinase and/or HMG-CoA reductase, as well ... 01/11/07 - 20070010540 - Crystal structure of liganded cfms kinase domain A crystal structure of the cfms kinase domain, co-crystal structure with a bound small molecule, as well as methods of using the same in the discovery of cfms inhibitors and in the treatment of diseases mediated by inappropriate cfms activity. ... 01/04/07 - 20070004764 - Nitrogen-containing aromatic derivatives a salt thereof, or a hydrate of the foregoing. ... 12/28/06 - 20060293355 - Crystalline form of bis [(e)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino] pyrimidin-5-yl] (3r,5s)-3, 5-dihydroxyhept-6-enoicacid] calcium salt Two polymorphic forms of bis[(E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl](3R,5S)-3,5-dihydroxyhept-6-enoic acid]calcium salt, processes for making them and their use as HMG Co-A reductase inhibitors are described. ... 12/28/06 - 20060293354 - Pyrimidine derivatives and their use as cb2 modulators The present invention relates to novel pyrimidine derivatives, pharmaceutical compositions containing these compounds and their use in the treatment of diseases, particularly pain, which diseases are caused directly or indirectly by an increase or decrease in activity of the cannabinoid receptor. ... 12/14/06 - 20060281774 - Pyrimidine derivatives for the treatment of abnormal cell growth wherein R1-R4 are as defined herein. Such novel pyrimidine derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. This invention also relates to a method of using such compounds in the treatment of abnormal cell growth in mammals, especially humans, and to pharmaceutical compositions ... 12/14/06 - 20060281773 - Inhibitors of the 11-beta-hydroxysteroid dehydrogenase type 1 enzyme The present invention relates to compounds which are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme for the treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome and other ... 11/30/06 - 20060270694 - Jak kinase inhibitors and their uses The present disclosure provides 2,4-pyrimidinediamine compounds that selectively inhibit JAK kinase as compared to Syk kinase and various methods of using the JAK-selective compounds. ... 11/23/06 - 20060264451 - Cxcr4 antagonists for the treatment of hiv infection The invention provides compounds, pharmaceutical compositions and methods of use of certain compounds that are antagonists of the chemokine CXCR4 receptor, and in particular to inhibit viral entry of certain viruses. Certain compounds in particular can reduce entry of immunodeficiency virus (HIV) into a cell while not reducing the capacity ... 11/16/06 - 20060258695 - Triazole derivatives as inhibitors of 11-beta hydroxysteroid dehydrogenase-1 Triazole derivatives of structural formula I are selective inhibitors of the 11β-hydroxysteroid dehydrogenase-1. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dyslipidemia, hyperlipidemia, hypertension, Metabolic Syndrome, and other symptoms associated with NIDDM. ... 11/02/06 - 20060247263 - Substituted heterocyclic compounds and methods of use and pharmaceutically acceptable salts and hydrates thereof. Also included is a method of treatment of inflammation, rheumatoid arthritis, Pagets disease, osteoporosis, multiple myeloma, uveititis, acute or chronic myelogenous leukemia, pancreatic β cell destruction, osteoarthritis, rheumatoid spondylitis, gouty arthritis, inflammatory bowel disease, adult respiratory distress syndrome (ARDS), psoriasis, Crohn's disease, allergic ... 11/02/06 - 20060247262 - 2,4 di (hetero) -arylamino-pyrimidine derivatives as zap-70 and/or syk inhibitors wherein R0, R1, R3 to R9, and Z have a signification as indicated in claim 1, which have interesting pharmaceutical properties. ... 11/02/06 - 20060247261 - Pyrimidine compounds The present invention relates to novel pyrimidine derivatives, pharmaceutical compositions containing these compounds and their use in the treatment of diseases, particularly pain, which diseases are caused directly or indirectly by an increase or decrease in activity of the cannabinoid receptor. ... 10/19/06 - 20060235036 - Vanilloid receptor ligands and their use in treatments and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic ... 10/12/06 - 20060229330 - 4-aminopyrimidine-5-one derivatives Novel intermediate compounds are disclosed. These compounds are useful in the synthesis of 4-aminopyrimidine-5-one derivatives that inhibit cyclin-dependent kinases, in particular cyclin-dependent kinase 4 (Cdk4). The 4-aminopyrimidine-5-one derivatives and their pharmaceutically acceptable salts have antiproliferative activity and are useful in the treatment or control of cancer, in particular solid tumors. ... 10/12/06 - 20060229329 - Pyrimidine derivatives possessing cell-cycle inhibitors activity Compounds of the formula (I), and pharmaceutically acceptable salts and in vivo hydrolysable esters thereof are described. Also described are processes for their preparation and their use as medicaments, particularly medicaments for producing a cell cycle inhibitory (anti cell proliferation) effect in a warm blooded animal, such as man. ... 10/12/06 - 20060229328 - 2-substituted pyrimidines R3 is cyano, CO2Ra, C(═O)NRzRb, C(═O)—N—ORb, C(═S)—NRaRb, C(═NORa)NRzRb, C(═NRa)NRzRb, C(═O)NRa—NRzRb, C(═N—NRzRc)NRaRb, C(═O)Ra, C(═NORb)Ra, C(═N—NRzRb)Ra, CRaRb—ORz, CRaRb—NRzRc, ON(═CRaRb), O—C(═O)Ra, NRaRb′, NRa(C(═O)Rb), NRa(C(═O)ORb), NRa(C(═O)—NRzRb), NRa(C(═NRc)Rb), NRa(N═CRcRb), NRa—NRzRb, NRz—ORa, NRa(C(═NRc)—NRzRb), NRa(C(═NORc)Rb), processes for preparing these compounds, compositions comprising these compounds and their pesticidal use are described. ... // - 2-Substituted pyrimidines of the formula I - ... 10/05/06 - 20060223837 - Biaryl derived amide modulators of vanilloid vr1 receptor The invention is directed to novel vanilloid receptor type 1 (VR1) ligands. More specifically, the invention relates to novel biaryl-derived amides that are potent antagonists or agonists of VR1. Pharmaceutical and veterinary compositions and methods of treating mild to severe pain and various diseases using compounds of the invention are ... 09/28/06 - 20060217404 - Pyridylpyrimidine derivatives as effective compounds against prion infections and prion diseases wherein R represents hydrogen or methyl and Z represents nitrogen containing functional groups, the use of the pyridylpyrimidine derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of prion infections and prion diseases, as well as compositions containing at least one pyridylpyrimidine derivative and/or pharmaceutically acceptable salt thereof. ... 09/14/06 - 20060205748 - Heterocyclic diamide invertebrate pest control agents This invention provides compounds of Formula (I), N-oxides and suitable salts thereof, wherein A and B are independently O or S; each J is independently a phenyl ring, a naphthyl ring system, a 5- or 6-membered heteroaromatic ring or an aromatic 8-, 9- or 10-membered fused heterobicyclic ring system wherein ... 09/07/06 - 20060199830 - N-(4-(4-methylthiazol-5-yl) pyrimidin-2-yl)-n-phenylamines as antiproliferative compounds The present invention relates to 2-substituted 4-heteroaryl-pyrimidines, 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 such as cancer, leukaemia, psoriasis and the like. ... 09/07/06 - 20060199829 - Inhibitors of histone deacetylase Disclosed are compounds of formula I that inhibit histone deacetylase (HDAC) enzymatic activity, pharmaceutical compositions comprising such compounds, as well as methods to treat conditions, particularly proliferative conditions, mediated at least in part by HDAC, wherein A, W, W1, W2, Ar2, and G are described herein. ... 08/10/06 - 20060178388 - Phenyl-substituted pyrimidine compounds useful as kinase inhibitors N, G, Z, R2, R3, R4, R5, and R6 are described in the specification. Also disclosed are pharmaceutical compositions containing compounds of formula (I), and methods of treating conditions associated with the activity of p38 kinase and/or conditions associated with the activity of LIM kinase. ... 07/13/06 - 20060154943 - Benzofuran derivatives and their use in the treatment of microbial infections The invention relates to new benzofuran derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as anti-infectives. ... 06/22/06 - 20060135543 - 2,4-pyrimidinediamine compounds and their uses The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized ... 06/22/06 - 20060135542 - Gtpase inhibitors and use thereof for controlling platelet hyperactivity The preferred embodiments generally relate to methods and compositions that affect the GTP-binding activity of members of the Rho family GTPases, preferably Rac (Rac1, Rac2 and/or Rac3), such compositions include compounds that modulate the GTP/GDP exchange activity, along with uses for the compounds including screening for compounds which recognize Rac ... 06/15/06 - 20060128735 - Substituted thiophenes with antibacterial activity Novel substituted thiophenes that are inhibitors of bacterial methionyl t-RNA synthetase (MRS) are disclosed. Also disclosed are method for their preparation and their use in therapy as anti-bacterial agents. ... 06/15/06 - 20060128734 - Diaryl urea derivatives useful for the treatment of protein kinase dependent diseases The invention relates to the use of diaryl urea derivatives in the treatment of protein kinase dependent diseases or for the manufacture of pharmaceutical compositions for use in the treatment of said diseases, methods of use of diaryl urea derivatives in the treatment of said diseases, pharmaceutical preparations comprising diaryl ... 06/08/06 - 20060122209 - Process for preparing trisubstituted pyrimidine compounds or a salt, solvate, clathrate, or prodrug thereof, wherein X, Y, R2, R3, R4, R7, R8, R9, R10, m and n are defined as within. ... 06/01/06 - 20060116391 - Process for preparing the calcium salt of rosuvastatin An improved process for manufacture of (E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl)(methylsulfonyl)amino]pyrimidin-5-yl](3R,5S)-3,5-dihydroxyhept-6-enoic acid calcium salt, which is useful for the production of a pharmaceutical useful in the treatment of, inter alia, hypercholesterolemia, hyperlipoproteinemia and atherosclerosis, is described. ... 05/25/06 - 20060111379 - Substituted 2-anilinopyrimidines as cell-cycle-kinase or receptor-tyrosine-kinase inhibitors, their production and use as pharmaceutical agents The present invention relates to a pharmaceutical composition comprising as active ingredient the hydrochloric acid salt of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino]benzonitrile and to processes for their preparation. ... 05/11/06 - 20060100227 - Pyrimidine derivaties Wherein X, R1, R2, R3, R4, R5, R6, R7, R8 and R9 are as indicated in claim 1, useful in disorders where ZAP-70 and/or Syk inhibition plays a role or caused by a malfunction of signal cascades connected with FAK. ... 05/04/06 - 20060094738 - Small molecules that replace or agonize p53 function This invention provides a novel screening system for identifying p53 mimetics/agonists. Also provided are small organic molecules that act as effective p53 mimetics/agonists. ... 04/13/06 - 20060079543 - Anilino-pyrimidine analogs wherein R1, R2, R3, R4, R5, and R6 are defined herein. ... 04/06/06 - 20060074097 - Regulation of mammalian keratinous tissue using hexamidine compositions A method of facilitating the cosmetic delivery of a hexamidine compound to keratinous tissue via a composition including the hexamidine compound, including the step of incorporating a thickening agent that is not negatively-charged into the composition. ... 04/06/06 - 20060074096 - 4-imidazolyl substituted pyrimidine derivatives with cdk inhibitory activity Compounds of the formula (I): wherein R1, R2, R3, R4, R5 and p are as defined within and a pharmaceutically acceptable salts and in vivo hydrolysable esters are described. Also described are processes for their preparation and their use as medicaments, particularly medicaments for producing a cell cycle inhibitory (anti-cell-proliferation) ... 03/30/06 - 20060069110 - Substituted heterocyclic compounds and methods of use The present invention relates to pyridines, pyrimidines and derivatives thereof, and pharmaceutically acceptable salts thereof. Also included is a method of treatment of inflammation, rheumatoid arthritis, Pagets disease, osteoporosis, multiple myeloma, uveititis, acute or chronic myelogenous leukemia, pancreatic β cell destruction, osteoarthritis, rheumatoid spondylitis, gouty arthritis, inflammatory bowel disease, adult ... 03/23/06 - 20060063790 - 4-arylspirocycloalkyl-2-aminopyrimidine carboxamide kcnq potassium channel modulators The invention encompasses compounds of Formula I, which are blockers of KCNQ channels. Blockers of KCNQ channels are known to enchance cognition in laboratory animals. The invention includes, salts, solvates, compositions, and methods of use. ... 02/23/06 - 20060040969 - Drug combinations comprising (e)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl] (3r,5s)-3,5-dihydroxyhept-6-enoic acid and an inhibitor, inducer or substrate of p450 isoenzyme 3a4 The invention concerns safe non-interacting drug combinations of a 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor, which is (E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl] (3R,5S)-3,5-dihydroxyhept-6-enoic acid or a pharmaceutically acceptable salt thereof (the Agent) and a drug which is either an inducer, inhibitor or a substrate of cytochrome P450, in particular cytochrome P450 isoenzyme 3A4. Particular ... 02/23/06 - 20060040968 - 2-(amino-substituted)-4-aryl pyrimidines and related compounds useful for treating inflammatory diseases A heterocyclic inhibitor having the formula I, with the variables defined herein, which is useful for treating inflammatory and other physiological disorders in which PKC-theta isoform plays a role: ... 02/16/06 - 20060035916 - 2,4-pyrimidinediamine compounds and their uses The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized ... 02/09/06 - 20060030576 - Anilinopyrimidine derivatives as ikk inhibitors and compositions and methods related thereto wherein R1 and R6 are as defined herein. Such compounds have utility in the treatment of a wide range of conditions that are responsive to IKK inhibition. Thus, methods of treating such conditions are also disclosed, as are pharmaceutical compositions containing one or more compounds of the above compounds. ... 02/09/06 - 20060030575 - Integrin alpha-v beta-3 antagonists for use in imaging and therapy Integrin receptor antagonists whose molecular structure includes a tetrahydropyridimidinylaminoethyloxybenzoyl group on a sulfonylamino-β-alanine nucleus exhibit increased binding affinity for the αvβ3 receptor when further substituted on the sulfonyl moiety with an N-amino alkycarbamyl group or a butyloxycarbonylamino alkylcarbamoyl group or similar groups. ... 01/05/06 - 20060004033 - Imidazolo-5-yl-2-anilino-pyrimidines as agents for the inhibition of the cell proliferation Compounds of the formula (I): wherein R1, R2, R3, R4, R5, R6, p, q, and n are as defined within and a pharmaceutically acceptable salts and in vivo hydrolysable esters are described. Also described are processes for their preparation and their use as medicaments, particularly medicaments for producing a cell ... 01/05/06 - 20060004032 - Gtpase inhibitors and methods of use The preferred embodiments generally relate to methods and compositions that affect the GTP-binding activity of members of the Rho family GTPases, preferably Rac (Rac1, Rac2 and/or Rac3), such compositions include compounds that modulate the GTP/GDP exchange activity, along with uses for the compounds including screening for compounds which recognize Rac ... 12/22/05 - 20050282847 - fungicidal 5-phenyl substituted 2-(cyanoamino) pyrimidines R1 and R5 together with the interjacent nitrogen atom form a heterocyclic ring; processes and intermediates for preparing these compounds, to compositions comprising them and to their use for controlling harmful fungi. ... 12/22/05 - 20050282846 - Compounds capable of activating cholinergic receptors Compounds incorporating aryl substituted olefinic amine are provided. Representative compounds are (4E)-N-methyl-5-(3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-pyrimidinyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-methoxy-3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(6-amino-5-methyl-3-pyridyl)-4-penten-2-amine, (2R)-(4E)-N-methyl-5-(3-pyridyl)-4-penten-2-amine, (2R)-(4E)-N-methyl-5-(5-isopropoxy-3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-bromo-3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-ethoxy-3-pyridyl)-4-penten-2-amine, (2S)-(4E)-N-methyl-5-(3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-isopropoxy-3-pyridyl)-4-penten-2-amine and (2S)-(4E)-N-methyl-5-(5-isopropoxy-3-pyridyl)-4-penten-2-amine. ... 12/22/05 - 20050282845 - Substituted pyrimidines as selective cyclooxygenase-2 inhibitors Methods for the treatment of pain, fever, inflammation of a variety of conditions and diseases. ... 12/22/05 - 20050282844 - 6,7-dihydro-5h-pyrazolo[1,2-a]pyrazol-1-ones which control inflammatory cytokines and pharmaceutical compositions thereof, and methods for controlling the level of one or more inflammation inducing cytokines selected from the group consisting of, interleukin-1 (IL-1), Tumor Necrosis Factor-α (TNF-α), interleukin-6 (IL-6), and interleukin-8 (IL-8), thereby controlling, mediating, or abating disease states affected by the level of extracellular inflammatory cytokines in ... 12/22/05 - 20050282843 - Therapeutic applications of 2-substituted 4-heteroarylpyrimidines R7 is a group (CH2)n—R8, wherein n is 0, 1, 2, 3 or 4 and wherein R8 is selected from alkyl, aryl, heteroaryl, heterocycloalkyl, F, Cl, Br, I, CF3, NO2, CN, OH, O-alkyl, O-aryl, O-heteroaryl, O-heterocycloalkyl, CO-alkyl, CO-aryl, CO-heteroaryl, CO-heterocycloalkyl, COO-alkyl, NH2, NH-alkyl, NH-aryl, N(alkyl)2, NH-heteroaryl, NH-heterocycloalkyl, COOH, CONH2, CONH-alkyl, ... 12/22/05 - 20050282842 - Therapeutic compounds based on pyrazolopyridine derivatives wherein all variables are as defined herein, pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceutical agents. ... 12/08/05 - 20050272753 - Diaminopyrimidinecarboxa mide derivative A compound which may be used for the prevention or treatment of respiratory diseases in which STAT 6 is concerned, particularly asthma, chronic obstructive pulmonary disease and the like is provided. A pyrimidine derivative or a salt thereof, which has an arylamino or arylethylamino group which may be substituted with ... 11/24/05 - 20050261324 - Pyrimidine hydantoin analogues which inhibit leukocyte adhesion mediated by vla-4 Disclosed are compounds which bind VLA-4 and/or LPAM-1. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4 and/or LPAM-1. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, ... 11/17/05 - 20050256145 - Pyrimidine derivatives for the treatment of abnormal cell growth wherein R1-R4 are as defined herein. Such novel pyrimidine derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. This invention also relates to a method of using such compounds in the treatment of abnormal cell growth in mammals, especially humans, and to pharmaceutical compositions ... 11/17/05 - 20050256144 - Pyrimidine derivatives for the treatment of abnormal cell growth wherein A and Ar are as defined herein. Such novel pyrimidine derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. This invention also relates to a method of using such compounds in the treatment of abnormal cell growth in mammals, especially humans, and to ... 11/03/05 - 20050245555 - Tri-substituted ureas as cytokine inhibitors The present invention relates to 1,1,3-tri-substituted ureas which inhibit the extracellular release of inflammatory cytokines, said cytokines responsible for one or more human or higher mammalian disease states. The present invention further relates to compositions comprising said 1,1,3-tri-substituted ureas which inhibit the extracellular release of inflammatory cytokines, and methods for ... 11/03/05 - 20050245554 - Substituted pyrimidines Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, ... 10/27/05 - 20050239811 - Tri-substituted ureas as cytokine inhibitors The present invention relates to 1,1,3-tri-substituted ureas which inhibit the extracellular release of inflammatory cytokines, said cytokines responsible for one or more human or higher mammalian disease states. The present invention further relates to compositions comprising said 1,1,3-tri-substituted ureas which inhibit the extracellular release of inflammatory cytokines, and methods for ... 10/20/05 - 20050234083 - Diamino-pyrimidines and their use as angiogenesis inhibitors Benzimidazole derivatives, which are useful as TIE-2 and/or VEGFR-2 inhibitors are described herein. The described invention also includes methods of making such benzimidazole derivatives as well as methods of using the same in the treatment of hyperproliferative diseases. ... 10/13/05 - 20050228005 - Protein kinase inhibitors and uses thereof or a pharmaceutically acceptable derivative or prodrug thereof, wherein A-B is N—O or O—N; Ar is an optionally substituted C5-10 aryl group; R1 is hydrogen or an optionally substituted group selected from C1-10 aliphatic, C5-10 aryl, C6-12 aralkyl, C3-10 heterocyclyl, or C4-12 heterocyclylalkyl; and T, n, R2 and R3 are ... 10/06/05 - 20050222186 - Substituted diaminopyrimidines The invention relates to substituted diaminopyrimidine compounds, which are effective therapeutic compounds for treating diseases and disorders associated with those commonly treated by Protein Kinase C theta (PKCθ) inhibitors. ... 09/22/05 - 20050209261 - Rho-kinase inhibitors Disclosed are compounds and derivatives thereof, their synthesis, and their use as Rho-kinase inhibitors. These compounds are useful for inhibiting tumor growth, treating erectile dysfunction, and treating other indications mediated by Rho-kinase, e.g., coronary heart disease. ... 09/22/05 - 20050209260 - Diaminopyrimidines as p2x3 and p2x2/3 antagonists or a pharmaceutically acceptable salt, solvate or prodrug thereof, wherein D, X, Y, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein. ... 09/22/05 - 20050209259 - Novel anhydrous amorphous forms of rosuvastatin calcium, pitavastatin calcium and fluvastatin sodium The present invention relates to novel anhydrous amorphous forms of bis[(E)[4-(4-fluorophenyl)isopropyl[methyl(methylsulfonyl)amino]pyrimidinyl](3R,5S)-3,5-dihydroxyhept enoic acid]calcium salt (rosuvastatin calcium), (±)7-(3-(4-fluorophenyl)-1-(1-methylethyl)-1H-indol-2-yl)3,5-dihydroxy heptenoic acid monosodium salt (fluvastatin sodium) and bis[(E)-3,5-dihydroxy-7-[4′-(4″-fluorophenyl)-2′-cyclopropyl-quinolin-3′-hept-6-enoic acid]calcium salt (pitavastatin calcium), to processes for their preparation, to pharmaceutical compositions containing them and to methods of treatment using the same. The rosuvastatin calcium, ... 09/22/05 - 20050209258 - Dithianon-based fungicidal mixtures in which R is methyl, cyclopropyl or 1-propynyl, in a synergistically effective amount, methods for controlling harmful fungi using mixtures of compounds I and II and the use of the compounds I and II for preparing such mixtures are described. ... 09/08/05 - 20050197354 - Hiv inhibiting pyrimidine derivatives the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein A is CH, CR4 or N; n is 0 to 4; Q is hydrogen or —NR1R2; R1 and R2 are selected from hydrogen, hydroxy, C1-12alkyl, C1-12alkyloxy, C1-12alkylcarbonyl, C1-12alkyloxycarbonyl, aryl, amino, mono- or di(C1-12alkyl)-amino, mono- or di(C1-12alkyl)aminocarbonyl ... 09/08/05 - 20050197353 - Indole derivatives or benzimidazole derivatives for modulating ikb kinase The present invention relates to indole derivatives or benzimidazole derivatives, to processes for preparing such compounds, to pharmaceutical compositions comprising such compounds, and methods for the prophylaxis and therapy of a disease associated with an increased activity of IκB kinase comprising administering such compounds. ... 09/01/05 - 20050192306 - Pyrimidine derivatives as selective inhibitors of cox-2 Methods of treating a subject suffering from a condition which is mediated by COX-2. ... 09/01/05 - 20050192305 - Hiv inhibiting pyrimidine derivatives the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein A is CH, CR4 or N; n is 0 to 4; Q is hydrogen or —NR1R2; R1 and R2 are selected from hydrogen, hydroxy, C1-12alkyl, C1-12alkyloxy, C1-12alkylcarbonyl, C1-12alkyloxycarbonyl, aryl, amino, mono- or di(C1-12alkyl)-amino, mono- or di(C1-12alkyl)aminocarbonyl ... 09/01/05 - 20050192304 - Rho-kinase inhibitors Disclosed are compounds and derivatives thereof, their synthesis, and their use as Rho-kinase inhibitors. These compounds are useful for inhibiting tumor growth, treating erectile dysfunction, and treating other indications mediated by Rho-kinase, e.g., coronary heart disease. ... 09/01/05 - 20050192303 - Pyrazolopyridinyl pyridine and pyrimidine therapeutic compounds wherein all variables are as defined herein, pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceutical agents. ... 09/01/05 - 20050192302 - 3-cycloalkylaminopyrrolidine derivatives as modulators of chemokine receptors (wherein R1, R2, R3, R4, R5, R6, R7, X, Y and Z are as defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of chemokine receptors and more specifically as modulators of the CCR2 and/or CCR5 receptor. The compounds and ... 08/25/05 - 20050187236 - Nitrogen-containing aromatic derivatives a salt thereof, or a hydrate of the foregoing. ... 08/18/05 - 20050182080 - Therapeutic compounds wherein all variables are as defined herein, pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceutical agents. ... 08/04/05 - 20050171134 - 4,5-disubstituted-2-aminopyrimidines R5 is a halogen atom or an alkynyl group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are selective KDR kinase and/or FGFr kinase inhibitors and are of use in the prophylaxis and treatment of disease states associated with angiogenesis ... 08/04/05 - 20050171133 - Therapeutic compounds wherein all variables are as defined herein, pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceutical agents. ... 08/04/05 - 20050171132 - Diaminopyrimidine derivatives as selective growth hormone secrectgogue receptor (ghs-r) antagonists or a therapeutically suitable salt or prodrug thereof, the preparation of the compounds, compositions containing the compounds and the use of the compounds in the prevention or treatment of disorders regulated by the action of ghrelin receptor, including Prader-Willi syndrome, eating disorder, weight gain, weight-loss maintainance following diet and exercise, ... 08/04/05 - 20050171131 - Diaminopyrimidine derivatives as growth hormone secrectgogue receptor (ghs-r) antagonists or a therapeutically suitable salt or prodrug thereof, the preparation of the compounds, compositions containing the compounds and the use of the compounds in the prevention or treatment of disorders regulated by the action of ghrelin receptor, including Prader-Willi syndrome, eating disorder, weight gain, weight-loss maintainance following diet and exercise, ... 07/28/05 - 20050165036 - Substituted benzofurans and benzothiophenes, methods of making and methods of use as integrin antagonists where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, m, n, i, j and k are defined herein. ... 07/21/05 - 20050159437 - Pharmaceutical agents wherein B is optionally substituted aryl; R1 and R2 are the same or different and are independently selected from hydrogen or C1-3 alkyl; n is 1 or 2, preferably n is 1; m is 0 or 1; R3 is hydrogen or acyl; R4 and R5 are the same or different ... 07/07/05 - 20050148613 - Carbonylamino-derivatives as novel inhibitors of histone deacetylase This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, R3, R4, R5, L, Q, X, Y and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine. ... 06/30/05 - 20050143405 - Pyridine and pyrimidine derivatives wherein R1, R2, R3, R4 and X are as defined in the specification, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with DPP IV, such as diabetes, particularly non-insulin dependent diabetes mellitus, and impaired glucose tolerance. ... 06/16/05 - 20050131002 - Novel amide compounds and medications containing the same R5 represents a hydrogen atom, a lower alkyl group, an aryl group or an optionally substituted silyl lower alkyl group, and n is an integer of from 1 to 15, or salts or solvates thereof, and a pharmaceutical composition containing at least one of these compounds. ... 06/16/05 - 20050131001 - Novel amide compounds and medications containing the same technical field R5 represents a hydrogen atom, a lower alkyl group, an aryl group or an optionally substituted silyl lower alkyl group, and n is an integer of from 1 to 15, or salts or solvates thereof, and a pharmaceutical composition containing at least one of these compounds. ... 06/16/05 - 20050131000 - Derivatives of 4-(imidazol-5-yl)-2-(4-sulfoanilino)pyrimidine with cdk inhibitory activity Compounds of the formula (I): wherein R1, R2, R3, R4, R5 and p are as defined within and a pharmaceutically acceptable salts and in vivo hydrolysable esters are described. Also described are processes for their preparation and their use as medicaments, particularly medicaments for producing a cell cycle inhibitory (anti-cell-proliferation) ... 06/16/05 - 20050130999 - Heteroaryl compounds which inhibit leukocyte adhesion mediated by alpha-4 integrins Disclosed are compounds which bind α4 integrins, where the α4 integrin is preferably VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by α4 integrins, where the α4 integrin is preferably VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a ... 06/09/05 - 20050124641 - Process for preparing chiral diol sulfones and dihydroxy acid hmg coa reductase inhibitors where R4a is preferably aryl such as phenyl, and R1a is preferably alkyl such as t-butyl, which are intermediates used in preparing HMG CoA reductase inhibitors. ... 06/09/05 - 20050124640 - Pyrimidine derivatives useful as inhibitors of pkc-theta wherein 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 relates to ... 06/02/05 - 20050119291 - Pyrimidine compounds Compounds of the formula (I) wherein R1, R2, R3, R4, R5, R6 and p are as defined within and a pharmaceutically acceptable salts and (in vivo hydrolysable esters are described. Also described are processes for their preparation and their use as medicaments, particularly medicaments for producing a cell cycle inhibitory ... 06/02/05 - 20050119290 - Heterocyclic compounds which inhibit leukocyte adhesion mediated by alpha4 integrins Disclosed are compounds which bind α4 integrins, preferably VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by α4 integrins, preferably VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, ... ### FreshPatents.com Support |