Chalcogen Bonded Directly To A Ring Carbon Of The 1,3-diazine Ring Patents (Class 514/259.5)
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Publication number: 20100204237Abstract: Compounds of Formula (1), pharmaceuticals containing the same, especially anti-HIV agents having anti viral activity, especially inhibitory activity against HIV integrase, wherein X represents either one of the following groups: (wherein, C ring is nitrogen-containing aromatic heterocyclic ring in which at least one atom in atoms neighboring the atom bound to the pyrimidine ring is unsubstituted nitrogen atom; R10 is hydrogen or lower alkyl; D ring is aryl or heteroaryl) Z1 and Z3 each is independently a single bond, O, S, S(?O) or SO2; Z2 is a single bond, lower alkylene or lower alkenylene; Ar is optionally substituted aryl or optionally substituted heteroaryl; R1 is lower alkyl, substituted lower alkyl or the like; R2 is a hydrogen atom or optionally substituted lower alkyl; or R1 and R2 may form, together with an adjacent atom, an optionally substituted heterocyclic ring, a pharmaceutically acceptable salt or a solvate thereof.Type: ApplicationFiled: April 21, 2010Publication date: August 12, 2010Inventors: Hidenori Mikamiyama, Minamo Iwata, Yoshiyuki Taoda
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Publication number: 20100190692Abstract: A method for recognizing and evaluating the presence and function of GnRH receptors on tumor cells originating in the brain and/or nervous system and/or the meninges and/or reactive neuroglia cells and/or primitive neuroectodermal tumor cells and/or on Kaposi sarcoma is provided. Furthermore a method for reducing degenerate GnRH-positive tumor cells and/or for decreasing cellular replication of the above GnRH-positive tumor cells comprising administering to a cell or to a subject a replication decreasing amount of a GnRH agonist and/or GnRH antagonist and/or an erythropoietin agonist, and/or a thrombopoietin agonist, and/or a endothelin antagonist and/or a gonadotropin inhibiting hormone agonist is also provided. Furthermore, a diagnostic kit for detecting GnRH receptors on tumor cells according to the present methods is disclosed.Type: ApplicationFiled: February 5, 2010Publication date: July 29, 2010Inventor: JOHANNES C. VAN GROENINGHEN
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Publication number: 20100168063Abstract: The present invention provides a compound of Formula I or a pharmaceutically acceptable derivative, salt or prodrug thereof. Further provided is a method of treatment or prophylaxis of a viral infection in a subject comprising administering to said subject an effective amount of a compound of Formula I or a pharmaceutically acceptable derivative, salt or prodrug thereof. A pharmaceutical composition or medicament comprising a compound of Formula I is also provided.Type: ApplicationFiled: December 21, 2007Publication date: July 1, 2010Applicant: Avexa LimitedInventors: Eric Dale Jones, Jonathan Alan Coates, David Ian Rhodes, John Joseph Deadman, Nicholas Andrew Vandegraff, Lisa Jane Winfield, Neeranat Thienthong, William Issa, Neil Choi, Katherine MacFarlane
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Publication number: 20100137321Abstract: The present invention relates to derivatives of imidazo[1,2-a]azines of formula I, in which R, R1 to R3, X, Y and n have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired. The invention further relates to processes for the preparation of compounds of formula I, to pharmaceutical compositions comprising them, and to the use of compounds of formula I for the stimulation of the expression of endothelial NO synthase or for the treatment of various diseases including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency, for example.Type: ApplicationFiled: August 27, 2009Publication date: June 3, 2010Applicant: SANOFI-AVENTISInventors: Gerhard ZOLLER, Hartmut STROBEL, David William WILL, Paulus WOHLFART
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Publication number: 20100113441Abstract: The invention relates to substituted imidazopyrimidines and triazolopyrimidines, to methods for the production thereof, and to the use of same for producing medicaments for the treatment and/or prophylaxis of diseases, especially haematological diseases, preferably leucopenia and neutropenia.Type: ApplicationFiled: March 4, 2008Publication date: May 6, 2010Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Stephan Siegel, Andreas Wilmen, Susanne Röhrig, Niels Svenstrup, Mark Jean Gnoth, Stefan Heitmeier, Ulrich Rester, Dmitry Zubov, Jochen Strayle, Michael Sperzel
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Publication number: 20090281121Abstract: The invention relates to a pyrimidone derivative represented by formula (I) or a salt thereof: Wherein X, Y, R1, R2, R3, R4, n, p, q, o and m are as described herein. The invention relates also to a medicament comprising the said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3?, such as Alzheimer disease.Type: ApplicationFiled: May 1, 2009Publication date: November 12, 2009Applicants: SANOFI-AVENTIS, MITSUBISHI TANABE PHARMA CORPORATIONInventors: Alistair LOCHEAD, Mourad SAADY, Franck SLOWINSKI, Philippe YAICHE
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Patent number: 7608624Abstract: The invention relates to a method of treatment of a variety of neurodegenerative diseases such as Alzheimer disease using a imidazo[1,2-a]pyrimidone derivative represented by formula (I) or a salt thereof: Wherein X, R1, R2, and n are as defined herein.Type: GrantFiled: March 8, 2006Date of Patent: October 27, 2009Assignees: Sanofi-Aventis, Mitsubishi Pharma Corporation TokyoInventors: Alistair Lochead, Severine Marguerie, Mourad Saady, Philippe Yaiche
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Publication number: 20090264420Abstract: The present invention provides a compound of formula I: said compound is inhibitor of aldosterone synthase, and/or 11 beta-hydroxylase (CYPL11B1), and/or aromatase, and thus can be employed for the treatment of a disorder or disease mediated by aldosterone synthase, aromatase, or CYPL11B1. Accordingly, the compound of formula I can be used in treatment of hypokalemia, hypertension, congestive heart failure, renal failure, in particular, chronic renal failure, restenosis, atherosclerosis, syndrome X, obesity, nephropathy, post-myocardial infarction, coronary heart diseases, increased formation of collagen, fibrosis and remodeling following hypertension and endothelial dysfunction. Finally, the present invention also provides a pharmaceutical composition.Type: ApplicationFiled: August 23, 2007Publication date: October 22, 2009Inventors: Gary Michael Ksander, Qi-Ying Hu
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Patent number: 7566720Abstract: The invention relates to therapeutic uses of a pyrimidone derivative represented by formula (I) or a salt thereof: Wherein X, Y, R1, R2, m and n are as defined herein. Specifically, a medicament comprising the said derivative or a salt thereof as an active ingredient is used for preventive and/or therapeutic treatment of a neurodegenerative diseases caused by abnormal activity of GSK3? such as Alzheimer's disease.Type: GrantFiled: August 20, 2007Date of Patent: July 28, 2009Assignees: Sanofi-Aventis, MItsubishi Pharma CorporationInventors: Antonio Almario Garcia, Thierry Gallet, Adrien Tak Li, Alistair Lochead, Severine Marguerie, Alain Nedelec, Mourad Saady, Philippe Yaiche
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Patent number: 7563797Abstract: The present invention relates to compounds of formula I, II, III or IV: wherein R1-R4, R7-R10, R13-R17 and R20-R24 are as described herein. The compounds are active as cannabinoid receptor ligands, e.g., CB2 ligands. Methods of preparing the compounds, compositions containing the compounds and methods of treatment using the compounds are also disclosed.Type: GrantFiled: August 27, 2007Date of Patent: July 21, 2009Assignee: Forest Laboratories Holding LimitedInventors: Gian-Luca Araldi, Matthew Ronsheim, Nhut K. Diep
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Patent number: 7504403Abstract: The present invention relates to pyrimidinones and pyridones 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 ? cell destruction, osteoarthritis, rheumatoid spondylitis, gouty arthritis, inflammatory bowel disease, adult respiratory distress syndrome (ARDS), psoriasis, Crohn's disease, allergic rhinitis, ulcerative colitis, anaphylaxis, contact dermatitis, asthma, muscle degeneration, cachexia, Reiter's syndrome, type I diabetes, type II diabetes, bone resorption diseases, graft vs.Type: GrantFiled: January 21, 2005Date of Patent: March 17, 2009Assignee: Amgen Inc.Inventors: Michael J. Frohn, Fang-Tsao Hong, Longbin Liu, Patricia Lopez, Aaron Siegmund, Seifu Tadesse, Nuria Tamayo
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Patent number: 7485640Abstract: The present invention discloses a compound of formula I, or a pharmaceutically acceptable salt thereof: (I) wherein —U—V— represents —CH?CH—, or —CH2—CH2—, —N?CH— or —CH?N—; X1 represents hydrogen, halogen, C1-6 alkyl, trifluoromethyl or C1-6 alkoxy; X2 represents hydrogen or halogen; Y represents a chemical bond, an oxygen atom, or a —NH— or —OCH2— linkage; Z represents an optionally substituted aryl or heteroaryl group; R1 represents hydrocarbon, a heterocyclic group, trifluoromethyl, —SO2Ra, —SO2NRaRb, —CORa, —CO2Ra or —CONRaRb; and Ra and Rb independently represent hydrogen, hydrocarbon or a heterocyclic group; pharmaceutical compositions comprising it; its use in methods of treatment; use of it in the manufacture of a medicament for treating and/or preventing anxiety; convulsions or a cognitive disorder; and methods of treatment using it.Type: GrantFiled: October 29, 2003Date of Patent: February 3, 2009Assignee: Merck Sharp & Dohme LimitedInventors: William Robert Carling, Jose Luis Castro Pineiro, Simon Charles Goodacre, David James Hallett, Leslie Joseph Street
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Publication number: 20080318980Abstract: The invention relates to a imidazo[1,2-a]pyrimidone derivative represented by formula (I) or a salt thereof: Wherein: X represents a bond, an ethenylene group, an ethynylene group, a methylene group optionally substituted; a carbonyl group, an oxygen atom, a sulfur atom, a sulfonyl group, a sulfoxide group or a nitrogen atom being optionally substituted; R1 represents a 2, 4 or 5-pyrimidinyl optionally substituted; R2 represents a C1-6 alkyl group, a C1-2 perhalogenated alkyl group, a C1-3 halogenated alkyl group, a benzyl group, a benzene ring, a naphthalene ring, 5,6,7,8-tetrahydronaphthalene ring, a pyridine ring, an indole ring, a pyrrole ring, a thiophene ring, a furan ring or an imidazole ring, the benzyl group and the rings being optionally substituted; and n represents 0 to 3.Type: ApplicationFiled: August 20, 2008Publication date: December 25, 2008Applicants: SANOFI-AVENTIS, MITSUBISHI PHARMA CORPORATIONInventors: Alistair LOCHEAD, Mourad SAADY, Philippe YAICHE
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Patent number: 7465737Abstract: The invention relates to use of a pyrimidone derivative represented by formula (I)or a salt thereof wherein: X, Y, R1, R2, R3, R4, R5, m, n and p are as defined herein. In particular, the invention relates to a medicament comprising the said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3? or GSK3? and cdk5/p25, such as Alzheimer disease.Type: GrantFiled: May 16, 2007Date of Patent: December 16, 2008Assignees: Sanofi-Aventis, Mitsubishi Pharma CorporationInventors: Alistair Lochead, Alain Nedelec, Mourad Saady, Philippe Yaiche
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Patent number: 7462621Abstract: The invention relates to an use of pyrimidone derivative represented by formula (I) or a salt thereof: wherein m, n, p, X, Y, R1, R2, R3, R4 and R5 are as defined herein for treating a variety of disease states. More specifically, the invention relates to a medicament comprising the said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3? or GSK3? and cdk5/p25, such as Alzheimer's disease.Type: GrantFiled: April 5, 2007Date of Patent: December 9, 2008Assignees: Sanofi-Aventis, Mitsubishi Pharma CorporationInventors: Thierry Gallet, Patrick Lardenois, Alistair Lochead, Severine Marguerie, Alain Nedelec, Mourad Saady, Franck Slowinski, Philippe Yaiche
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Patent number: 7452892Abstract: The present application describes compounds according to both Formulas I and II, pharmaceutical compositions comprising at least one compound according to either Formula I or II and optionally one or more additional therapeutic agents, and methods of treatment using the compounds according to Formulas I and II both alone and in combination with one or more additional therapeutic agents. The compounds have the following general formulas: including all prodrugs, solvates, pharmaceutically acceptable salts and stereoisomers, wherein R1, R2, R3, R4 and R5 are described herein.Type: GrantFiled: June 16, 2006Date of Patent: November 18, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Gang Wu, Amarendra B. Mikkilineni, Philip M. Sher, Natesan Murugesan, Zhengxiang Gu
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Publication number: 20080280886Abstract: Disclosed herein are urea-based 5-HT receptor modulators, pharmaceutically acceptable salts and prodrugs thereof, the chemical synthesis thereof, and medical use of such compounds for the treatment and/or management of 5-HT receptor-mediated disorders.Type: ApplicationFiled: May 8, 2008Publication date: November 13, 2008Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Thomas G. Gant, Sepehr Sarshar
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Publication number: 20080267867Abstract: A method for inhibiting microbial growth comprises administering an effective amount of a silver complex of a N-heterocyclic amine. A method for treating cancer cells or a method for imaging one or more tissues of a patient includes administering an effective amount of a complex of a N-heterocyclic amine and a radioactive metal. N-heterocyclic carbenes of the present invention may be represented by formula (I) wherein Z is a heterocyclic group, and R1 and R2 are, independently or in combination, hydrogen or a C1-C12 organic group selected from the group consisting of alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, aryl, arylalkyl, alkylaryl, heterocyclic, and alkoxy groups and substituted derivatives thereof.Type: ApplicationFiled: September 7, 2004Publication date: October 30, 2008Inventors: Wiley J. Youngs, Claire A. Tessier, Jared Garrison, Carol Quezada, Abdulkareem Melaiye, Matthew Panzner, Semih Durmus
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Publication number: 20080214577Abstract: This invention relates to novel compounds having the structural formula I below: and to their pharmaceutically acceptable salt, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer Disease, neurodegeneration and dementia.Type: ApplicationFiled: June 11, 2007Publication date: September 4, 2008Applicants: AstraZeneca AB, Astex Therapeutics LtdInventors: Stefan Berg, Jorg Holenz, Katharina Hogdin, Karin Kolmodin, Niklas Plobeck, Didier Rotticci, Fernando Sehgelmeble, Maria Wirstam
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Publication number: 20080200479Abstract: The invention relates to new salts of ocaperidone and uses thereof, particularly in the pharmaceutical industry. The invention discloses specific salts of ocaperidone having increased water solubilities, as well as therapeutic methods by administering said salts, in particular for treating various diseases of the central or peripheral nervous system, especially central nervous system. It further deals with pharmaceutical compositions comprising said salts and methods for preparing the same.Type: ApplicationFiled: February 24, 2006Publication date: August 21, 2008Inventors: Stefano Biondi, Arnold Demailly, Cesare Mondadori, Jean-Laurent Paparin
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Publication number: 20080118559Abstract: Pharmaceutical compositions suitable for oral administration in solid dosage forms are described. The compositions comprise an effective amount of a drug compound in the form of a salt, wherein the drug salt is characterized by conversion to a less soluble form of the drug compound under certain pH conditions, and an anti-nucleating agent.Type: ApplicationFiled: December 2, 2005Publication date: May 22, 2008Inventors: Maria T. Cruanes, Wei Xu, Laura M. Artino, Honggang Zhu
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Patent number: 7294632Abstract: The invention relates to a dihydrospiro-[cycloalkyl]-pyrimidone derivative represented by formula (I) or a salt thereof: wherein X, Y, R1, R2, R3, m, n, p and q are as described herein. The invention relates also to a medicament comprising the said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3?, such as Alzheimer disease.Type: GrantFiled: September 7, 2005Date of Patent: November 13, 2007Assignees: Sanofi-Aventis, Mitsubishi Pharma CorporationInventors: Pascal George, Alistair Lochead, Mourad Saady, Franck Slowinski, Philippe Yaiche
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Patent number: 7173022Abstract: The invention encompasses a series cyclic bicyclic heterocyclic compounds of Formula I which are inhibitors of HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS.Type: GrantFiled: May 26, 2005Date of Patent: February 6, 2007Assignee: Bristol-Myers Squibb CompanyInventors: B. Narasimhulu Naidu, Jacques Banville, John D. Matiskella, Serge Plamondon, Yasutsugu Ueda
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Patent number: 7125863Abstract: Compounds according to formula (1), wherein R1 is H or CN, X1 is S, O, SO2 or CH2, X2 is CO, CH2 or a covalent bond, Het is a nitrogen-containing heterocycle and n is 1–5 are new. The compounds of the invention are inhibitors of dipeptidyl peptidase IV.Type: GrantFiled: April 26, 2001Date of Patent: October 24, 2006Assignee: Ferring BVInventors: David Michael Evans, Gary Robert William Pitt
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Patent number: 7067521Abstract: The invention relates to an imidazo[1,2-a]pyrimidone derivative represented by formula (1) or a salt thereof, wherein: X represents a bond, an ethenylene group, and ethenylene group, a methylene group optionally substituted by one or two groups selected from a C1-6 alkyl group, a hydroxy group and a C1-4 alkoxy group; a carbonyl group, an oxygen atom, a sulfur atom, a sulfonyl group, a sulfoxide group or a nitrogen atom being optionally substituted by a C1-6 alkyl group; R1 represents a 2,3 or 4-pyridyl group optionally substituted by a C1-4 alkyl group, C1-4 alkoxy group or a halogen atom; R2 represents a C1-6 alkyl group, a C1-2 perhalogenated alkyl group, a C1-3 halogenated alkyl group, a benzyl group, a phenyl ring, a naphthyl ring, 5,6,7,8-tetrahydronaphthyl ring, a pyridyl ring, an indole ring, a pyrrole ring, a thiophene ring, a furan ring or an imidazole ring, the benzyl group and the rings being optionally substituted by 1 to 4 substituents selected from a C1-6 alkyl group, a phenyl ring, a halogen aType: GrantFiled: August 31, 2001Date of Patent: June 27, 2006Assignee: sanofi-aventisInventors: Alistair Lochead, Séverine Marguerie, Mourad Saady, Philippe Yaiche
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Patent number: 6995154Abstract: The invention provides compounds of formula I: wherein R1 to R5 have any of the values defined in the specification, as well as pharmaceutically acceptable salts of the compounds, pharmaceutical compositions comprising the compounds, and methods of using the compounds, compositions, or salts to treat cancer. In embodiments, R4 and R5 taken together can be a 3, 4, or 5 membered saturated or unsaturated chain comprising members selected from the group consisting of non-peroxide oxygen, sulfur, N(X), and carbon, optionally substituted by oxo; wherein each X is independently absent or is H, O, (C1–C4)alkyl, phenyl or benzyl; and wherein at least one of the chain members is an N—H group.Type: GrantFiled: October 21, 2003Date of Patent: February 7, 2006Assignee: Rutgers, The State University of New JerseyInventors: Edmond J. LaVoie, Jung Sun Kim, Leroy Fong Liu
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Patent number: 6974819Abstract: Imidazo[1,2-?]pyrimidinones and pyrimido[1,2-?]pyrimidinones useful for preventive and/or therapeutic treatment of neurodegenerative diseases, such as Alzheimer's disease, caused by abnormal GSK3? activity.Type: GrantFiled: August 31, 2001Date of Patent: December 13, 2005Assignees: Sanofi-Aventis, Mitsubishi Pharma CorporationInventors: Antonio Almario Garcia, Thierry Gallet, Adrien Tak Li, Alistair Lochead, Séverine Marguerie, Alain Nedelec, Mourad Saady, Philippe Yaiche
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Patent number: 6921762Abstract: Selected novel substituted indolizine-like compounds are effective for treatment of diseases, such as TNF-?, IL-1?, IL-6 and/or IL-8 mediated diseases, and other maladies, such as cancer, pain and diabetes. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for treatment of diseases and other maladies or conditions involving inflammation, cancer, pain, diabetes and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: GrantFiled: November 15, 2002Date of Patent: July 26, 2005Assignee: Amgen Inc.Inventors: Guolin Cai, Jennifer N. Chau, Celia Dominguez, Yuelie Lu, Gilbert M. Rishton
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Patent number: 6911443Abstract: A compound of the formula (I) in which R1 is —OR11, —SR11, —SOR11, —SO2R11, —NHR11, or —NR12R13 , and R11, R12, and R13 are as defined broadly in the text. R2 is H, C1-C6alkyl, carbamoyl, or an ester group. R3 is thienyl, pyridyl optionally substituted by halogen or C1-C6alkoxy; naphthyl optionally substituted by C1-C6alkoxy; dioxane fused phenyl; dioxacyclopentane fused phenyl; or optionally substituted phenyl. Y is CH or N. A process for preparing such compounds, pharmaceutical compositions containing such compounds, and a method of treating asthma using them are also disclosed and claimed.Type: GrantFiled: April 17, 2001Date of Patent: June 28, 2005Assignee: Bayer AktiengesellschaftInventors: Takeshi Yura, Arnel B. Concepcion, Gyoonhee Han, Makiko Marumo, Hiroko Yoshino, Norihiro Kawamura, Toshio Kokubo, Hiroshi Komura, Yingfu Li, Timothy B. Lowinger, Muneto Mogi, Noriyuki Yamamoto, Nagahiro Yoshida, Scott Miller, Margaret A. Popp, Aniko M. Redmann, Martha E. Rodriguez, William J. Scott, Ming Wang
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Publication number: 20040266765Abstract: GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women.Type: ApplicationFiled: April 13, 2004Publication date: December 30, 2004Applicant: Neurocrine Biosciences, Inc.Inventors: Joseph Pontillo, Chen Chen
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Patent number: 6828326Abstract: The present invention relates to fused bicyclic metalloproteinase inhibitors of the formula wherein A, B, X, Y, and R1 are as defined in the specification, and to pharmaceutical compositions and methods of treating arthritis, inflammation, cancer and other disorders.Type: GrantFiled: August 5, 2003Date of Patent: December 7, 2004Assignee: Warner-Lambert CompanyInventors: Joseph Armand Picard, Michael William Wilson
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Publication number: 20040142942Abstract: GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women.Type: ApplicationFiled: October 20, 2003Publication date: July 22, 2004Inventors: Yun-Fei Zhu, Keith M. Wilcoxen, R. Scott Struthers, Chen Chen, Patrick J. Connors, Yinghong Gao, Fabio C. Tucci
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Publication number: 20040142928Abstract: The present invention provides a compound of formula I 1Type: ApplicationFiled: December 23, 2003Publication date: July 22, 2004Inventors: Gordon L. Bundy, Fred L. Ciske, Michael J. Genin, Steven E. Heasley, Scott D. Larsen, Byung Hyun Lee, Paul D. May, John R. Palmer, Mark E. Schnute, Valerie A. Vaillancourt, Atli Thorarensen, Allison J. Wolf, Nancy Anne Wicnienski, David Wilhite
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Publication number: 20040138236Abstract: A class of 3-phenylimidazo[1,2-c]pyrimidine derivatives, substituted at the meta position of the phenyl ring by an optionally substituted aryl or heteroaryl group which is directly attached or bridged by an oxygen atom or a —NH— linkage, are selective ligands for GABAA receptors, in particular having good affinity for the &agr;2 and/or &agr;3 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety and convulsions.Type: ApplicationFiled: May 7, 2003Publication date: July 15, 2004Inventors: David James Hallett, Michael Geoffrey Neil Russell, Leslie Joseph Street
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Publication number: 20040087598Abstract: The invention relates to pyrimidone derivative represented by formula (I) or a salt thereof wherein X represents hydrogen atoms, a sulfur atom, an oxygen atom or a C1-2 alkyl group and a hydrogen atom; Y represents a bond, an ethenylene group, an ethynylene group, a 1,2-cyclopropylene, an oxygen atom, a sulfur atom, a sulfonyl group, a sulfoxyde group, a carbonyl group, a nitrogen atom being optionally substituted; or a methylene group optionally substituted; R1 represent a 2,3 or 4-pyridyl group optionally substituted by a C3-6cycloalkyl group a C1-4alkyl group, a C1-4alkoxy group, a benzyl group or a halogen atom; when Y represents a bond, a methylene group optionally substituted or a carbonyl group then R2 represent a C1-16alkyl group, a C3-6cycloalkyl group, a C1-4alkylthio group, a C1-4alkoxy group, a C1-2perhalogenated alkyl group, a C1-3halogenated alkyl group, a 5,6,7,8-tetrahydronaphthyl ring, a naphthyl ring, a phenylthio group, a benzyl group, a phenyl ring, a pyridyl ring, an indole ring, a pyrrolType: ApplicationFiled: June 17, 2003Publication date: May 6, 2004Inventors: Antonio Almario Garcia, Thierry Gallet, Adrien Tak Li, Alistair Lochead, Severin Marguerie, Alain Nedelec, Mourad Saady, Philippe Yaiche
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Publication number: 20040044010Abstract: The invention relates to an imidazo[1,2-a]pyrimidone derivative represented by formula (1) or a salt thereof, wherein: X represents a bond, an ethenylene group, and ethenylene group, a methylene group optionally substituted by one or two groups selected from a C1-6 alkyl group, a hydroxy group and a C1-4 alkoxy group; a carbonyl group, an oxygen atom, a sulfur atom, a sulfonyl group, a sulfoxide group or a nitrogen atom being optionally substituted by a C1-6 alkyl group; R1 represents a 2,3 or 4-pyridyl group optionally substituted by a C1-4 alkyl group, C1-4 alkoxy group or a halogen atom; R2 represents a C1-4 alkyl group, perhalogenated alkyl group, a C1-3 halogenated alkyl group, a benzyl group, a phenyl ring, a naphthyl ring, 5,6,7,8-tetrahydronaphthyl ring, a pyridyl ring, an indole ring, a pyrrole ring, a thiophene ring, a furan ring or an imidazole ring, the benzyl group and the rings being optionally substituted by 1 to 4 substituents selected from a C1-4 alkyl group, a phenyl ring, a halogeType: ApplicationFiled: June 23, 2003Publication date: March 4, 2004Inventors: Alistair Lochead, Severine Marguerie, Mourad Saady, Philippe Yaiche
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Publication number: 20040014763Abstract: Compounds having the following structure: 1Type: ApplicationFiled: February 14, 2003Publication date: January 22, 2004Applicant: Myriad Pharmaceuticals, Inc.Inventors: Cyprian O. Ogbu, Hwa-Ok Kim, Mark A. Blaskovich
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Publication number: 20040006065Abstract: The present invention relates generally to compounds that inhibit serine proteases.Type: ApplicationFiled: June 19, 2003Publication date: January 8, 2004Inventor: Peter W. Glunz
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Patent number: 6667302Abstract: The invention provides compounds of formula I: wherein R1 to R5 have any of the values defined in the specification, as well as pharmaceutically acceptable salts of the compounds, pharmaceutical compositions comprising the compounds, and methods of using the compounds, compositions, or salts to treat cancer. In embodiments, R4 and R5 taken together can be a 3, 4, or 5 membered saturated or unsaturated chain comprising members selected from the group consisting of non-peroxide oxygen, sulfur, N(X), and carbon, optionally substituted by oxo; wherein each X is independently absent or is H, 0, (C1-C4)alkyl, phenyl or benzyl; and wherein at least one of the chain members is an N—H group.Type: GrantFiled: June 13, 2001Date of Patent: December 23, 2003Assignee: Rutgers, The State University of New JerseyInventors: Edmond J. La Voie, Jung Sun Kim, Leroy Fong Liu
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Patent number: 6653295Abstract: The present invention relates generally to a novel class of pyrimidinones of Formula (I): that are useful as serine protease inhibitors, and more particularly as Hepatitis C virus NS3 protease inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of using the same.Type: GrantFiled: December 12, 2001Date of Patent: November 25, 2003Assignee: Bristol-Myers Squibb CompanyInventors: Peter William Glunz, Brent Dale Douty, Wei Han
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Publication number: 20030216411Abstract: GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women.Type: ApplicationFiled: January 28, 2003Publication date: November 20, 2003Applicant: Neurocrine Biosciences, Inc.Inventors: Yun-Fei Zhu, Timothy D. Gross, Ying Hing Gao, Patrick J. Connors, Zhiqiang Guo, Chen Chen
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Patent number: 6649604Abstract: Selected novel substituted pyrimidinone and pyridone compounds are effective for prophylaxis and treatment of diseases, such as TNF-&agr;, IL-1&bgr;, IL-6 and/or IL-8 mediated diseases, and other maladies, such as pain and diabetes. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving inflammation, pain, diabetes and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: GrantFiled: April 23, 2002Date of Patent: November 18, 2003Assignee: Amgen Inc.Inventors: Ulrike D. Spohr, Michael J. Malone, Nathan B. Mantlo, Jeffrey A. Zablocki
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Publication number: 20030207880Abstract: The present invention provides a compound of formula I 1Type: ApplicationFiled: December 18, 2002Publication date: November 6, 2003Inventors: Gordon L. Bundy, Fred L. Ciske, Michael J. Genin, Steven E. Heasley, Scott D. Larsen, Byung Hyun Lee, Paul D. May, John R. Palmer, Mark E. Schnute, Valerie A. Vaillancourt, Atli Thorarensen, Allison J. Wolf, Nancy Anne Wicnienski, David Wilhite
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Publication number: 20030119848Abstract: 1Type: ApplicationFiled: August 7, 2002Publication date: June 26, 2003Inventors: Makoto Takemura, Hisashi Takahashi, Katsuhiro Kawakami, Kenji Namba, Mayumi Tanaka, Rie Miyauchi
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Publication number: 20030114458Abstract: The present invention provides compounds of Formula (I): 1Type: ApplicationFiled: May 29, 2002Publication date: June 19, 2003Inventors: Edmund Lee Ellsworth, Howard Daniel Hollis Showalter
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Publication number: 20030109535Abstract: GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women.Type: ApplicationFiled: August 2, 2002Publication date: June 12, 2003Applicant: Neurocrine Biosciences, Inc.Inventors: Joseph Pontillo, Chen Chen
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Publication number: 20030073704Abstract: Selected novel substituted pyrimidinone and pyridone compounds are effective for prophylaxis and treatment of diseases, such as TNF-&agr;, IL-1&bgr;, IL-6 and/or IL-8 mediated diseases, and other maladies, such as pain and diabetes. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving inflammation, pain, diabetes and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: ApplicationFiled: April 23, 2002Publication date: April 17, 2003Applicant: Amgen Inc.Inventors: Ulrike D. Spohr, Michael J. Malone, Nathan B. Mantlo, Jeffery A. Zablocki
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Publication number: 20030064962Abstract: The present invention relates generally to a novel class of pyrimidinones of Formula (I): 1Type: ApplicationFiled: December 12, 2001Publication date: April 3, 2003Inventors: Peter William Glunz, Brent Dale Douty, Wei Han
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Patent number: 6537998Abstract: GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein Ar, A, B, Q, R1, R2, R3a, R3b, R6, R7 and m are as defined herein, including stereoisomers, prodrugs and pharmaceutical 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 for antagonizing gonadotropin-releasing hormone in a subject in need thereof.Type: GrantFiled: October 16, 2000Date of Patent: March 25, 2003Assignee: Neurocrine Biosciences, Inc.Inventors: Yun-Fei Zhu, Timothy D. Gross, Yinghong Gao, Patrick J. Connors, Jr., Zhiqiang Guo, Chen Chen
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Patent number: 6489333Abstract: This invention relates to novel heterocycles which are useful as antagonists of the &agr;v&bgr;3 integrin, the &agr;2b&bgr;3 integrin, and related cell surface adhesive protein receptors, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of cell adhesion, the treatment of angiogenic disorders, inflammation, bone degradation, cancer metastasis, diabetic retinopathy, thrombosis, restenosis, macular degeneration, and other conditions mediated by cell adhesion and/or cell migration and/or angiogenesis.Type: GrantFiled: April 9, 2001Date of Patent: December 3, 2002Assignee: Bristol - Meyers Squibb Pharma CompanyInventors: William J. Pitts, Prabhakar K. Jadhav