The Nitrogen Is Part Of A Hetero Ring Patents (Class 514/273)
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Publication number: 20120095001Abstract: The present invention relates to substituted 1,3,8-triazaspiro[4.5]decame-2,4-diones useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.Type: ApplicationFiled: June 7, 2010Publication date: April 19, 2012Applicant: Merck Sharp & Dohme Corp.Inventors: Joan M. Pierce, Jeffrey J. Hale, Shouwu Miao, Petr Vachal
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Publication number: 20120059014Abstract: The present invention is directed to therapeutic compounds of the following formula (I) which have activity as agonists of GPR119 and are useful for the treatment of metabolic disorders including type II diabetes.Type: ApplicationFiled: March 12, 2010Publication date: March 8, 2012Applicant: PROSIDION LIMITEDInventors: Oscar Barba, Tom Banksia Dupree, Peter Timothy Fry, Matthew Colin Thor Fyfe, Revathy Perpetua Jeevaratnam, Thomas Martin Krulle, Karen Lesley Schofield, Donald Smyth, Thomas Staroske, Alan John William Stewart, David French Stonehouse, Simon Andrew Swain, David Matthew Withall
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Publication number: 20120010183Abstract: The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to a new sulfonamide Nav1.7 inhibitors of formula (I): or a pharmaceutically acceptable salt thereof, wherein Het1, X, R1, R2, R3, R4 and R5 are as defined in the description. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.Type: ApplicationFiled: July 11, 2011Publication date: January 12, 2012Applicant: PFIZER LIMITEDInventors: Andrew Simon Bell, Alan Daniel Brown, Marcel John De Groot, Russell Andrew Lewthwaite, Ian Roger Marsh, David Simon Millan, Manuel Perez Pacheco, David James Rawson, Nunzio Sciammetta, Robert Ian Storer, Nigel Alan Swain, Steven Matthieu Gaulier
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Publication number: 20110257152Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein R1a, R1b, R1c, X, and Y are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as Cdc7 and methods of treating diseases such as cancer.Type: ApplicationFiled: April 14, 2011Publication date: October 20, 2011Applicant: ABBOTT LABORATORIESInventors: Thomas D. Penning, Keith W. Woods, Chunqiu Lai, Yunsong Tong, Alan S. Florjancic
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Publication number: 20110245227Abstract: Novel compounds are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. These novel compounds have the structure Formula I or Formula IA.Type: ApplicationFiled: June 14, 2011Publication date: October 6, 2011Inventors: Dean A. Wacker, Karen A. Rossi, Ying Wang
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Publication number: 20110207733Abstract: The invention encompasses pyrimidine derivatives as gamma secretase modulators, useful for treating diseases associated with the deposition of beta-amyloid peptide in the brain, such as Alzheimer's disease, or of preventing or delaying the onset of dementia associated with such diseases. Pharmaceutical compositions and methods of use are included.Type: ApplicationFiled: July 31, 2009Publication date: August 25, 2011Inventors: Alexey A. Rivkin, Sean P. Ahearn, Stephanie M. Chichetti
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Publication number: 20110190298Abstract: The present invention provides compounds of Formula I, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent; diseases or disorders associated with the activity of GPR119.Type: ApplicationFiled: July 9, 2009Publication date: August 4, 2011Applicant: IRM LLCInventors: Robert Epple, Gerald Lelais, Victor Nikulin
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Publication number: 20110166109Abstract: The present invention relates to novel active compound combinations comprising, firstly, at least one known compound of the formula (I) in which R1 and R2 have the meanings given in the description. and at least one further known active compound from groups (2) to (27) listed in the description, which combinations are highly suitable for controlling animal pests such as insects and unwanted acarids and also phytopathogenic fungi.Type: ApplicationFiled: July 15, 2010Publication date: July 7, 2011Applicant: Bayer CropScience AGInventors: Wolfram Andersch, Heike Hungenberg
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Publication number: 20110065706Abstract: A compound of formula I or a pharmaceutically acceptable salt thereof, processes for preparing such compounds, their use as GPR119 modulators, methods for their therapeutic use, particularly in the treatment of obesity and diabetes mellitus, and pharmaceutical compositions containing them.Type: ApplicationFiled: September 10, 2010Publication date: March 17, 2011Applicant: AstraZeneca ABInventors: Alan Martin Birch, Roger John Butlin, David Stephen Clarke, Andrew Leach, Philip Alexander MacFaul, Charles John O'Donnell, James Stewart Scott, Paul Robert Owen Whittamore, Dan Anders Broo, Öjvind Percy Davidsson, Kjell Erik Johansson, Hanna De La Motte
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Publication number: 20100292205Abstract: The invention pertains to pyrimidone compounds that serve as effective GSK-3 inhibitors. The invention further relates to pharmaceutical compositions and methods comprising such pyrimidone compounds; and the use of such compounds for treating certain disorders.Type: ApplicationFiled: August 13, 2007Publication date: November 18, 2010Applicant: PFIZER INC.Inventors: Bruce A. Lefker, Michael A. Brodney, Subas M. Sakya, Bruce A. Hay, Matthew D. Wessel, Edward L. Conn
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Patent number: 7776864Abstract: Compounds of formula (I) a tautomer or stereoisomer thereof, or a salt thereof, wherein ring B and the pyrimidine to which it is fused, R4, R5, R6 and R7 have the meanings as given in the description and the claims, are effective inhibitors of the Pi3K/Akt pathway.Type: GrantFiled: August 14, 2008Date of Patent: August 17, 2010Assignee: Bayer Schering Pharma AGInventors: Swen Hölder, Matthias Vennemann, Gerrit Beneke, Armin Zülch, Volker Gekeler, Thomas Beckers, Astrid Zimmermann, Hemant Joshi
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Publication number: 20100203001Abstract: The present invention relates to an improved method of formation of disulfide bridges in substances bearing SH groups, in particular peptides, for example by formation of intramolecular disulfide bridges, in which a heterocyclic compound having at least one nitrogen atom (e.g. caffeine or a caffeine-like substance) is used for catalysis of the reaction. It was found, surprisingly, that addition of the heterocyclic substance increases both the yield and the purity of the product bearing disulfide bridges.Type: ApplicationFiled: December 21, 2007Publication date: August 12, 2010Applicant: APLAGEN GMBHInventors: Karsten Knorr, Marco Emgenbroich, Carsten Büngener
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Publication number: 20100093775Abstract: Compounds represented by formula I: or pharmaceutically acceptable salts and solvates thereof, wherein R1, X, Y, Y1, and Z are as defined herein, are useful for treating flaviviridae viral infections.Type: ApplicationFiled: July 24, 2009Publication date: April 15, 2010Applicant: VIROCHEM PHARMA INC.Inventors: Real DENIS, Carl Poisson, Sanjoy Kumar Das, Irina Motorina, Rabindra Rej, Constatin G. Yannopoulos, Laval Chan Chun Kong
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Publication number: 20100016319Abstract: This invention relates to a pharmaceutical comprising as an effective ingredient an arylmethylene urea exemplified by the following formula: or a pharmaceutically acceptable salt thereof. The arylmethylene urea and the pharmaceutically acceptable salts thereof are useful for therapy or prophylaxis of inflammatory bowel disease and overactive bladder.Type: ApplicationFiled: November 29, 2006Publication date: January 21, 2010Applicant: TORAY INDUSTRIES, INC. a corporation of JapanInventors: Michihiro Ohno, Hideki Inoue, Shinnosuke Hayashi, Mie Kaino, Sunao Hara, Satoru Yoshikawa
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Publication number: 20090286791Abstract: The present invention provides compounds represented by the formula (Ia): the formula (Ib): the formula (Ic): and the formula (Id): wherein each symbol is as defined in the specification. According to the present invention, these compounds have a DGAT inhibitory activity and are useful for the prophylaxis, treatment or improvement of diseases or pathologies caused by high expression or high activation of DGAT.Type: ApplicationFiled: July 20, 2007Publication date: November 19, 2009Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Shuji Kitamura, Thomas Daniel Aicher, Steve Gonzales, Yvan Le Huerou, Scott Alan Pratt, Tim Turner, Yoshihisa Nakada
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Publication number: 20090233918Abstract: A compound represented by the formula (I), an optically active isomer thereof, or a pharmaceutical acceptable salt thereof: wherein R2 represents a hydrogen or the like; R3 represents methyl group or the like; R20 represents a halogen atom or the like; q represents an integer of 0 to 3; Z represent nitrogen atom, CH, or the like; R4 represents hydrogen or the like; R5 represents hydrogen or the like; R6 represents a substituted alkyloxy and the like; p represents an integer of 0 to 3; X represents bond, CH2, oxygen atom, NH, or the like; any one or more of R5 and R6, R5 and R4, R6 and R4, X and R5, X and R4, X and R6, and R6 and R6 may combine to each other to form a ring, which is used for preventive and/or therapeutic treatment of a disease caused by tau protein kinase 1 hyperactivity such as a neurodegenerative diseases (e.g. Alzheimer disease).Type: ApplicationFiled: March 14, 2007Publication date: September 17, 2009Applicants: MITSUBISHI TANABE PHARMA CORPORATION, SANOFI-AVENTISInventors: Kenji Fukunaga, Toshiyuki Kohara, Kazutoshi Watanabe, Yoshihiro Usui, Fumiaki Uehara, Satoshi Yokoshima, Daiki Sakai, Shin-ichi Kusaka, Kazuki Nakayama
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Publication number: 20090181992Abstract: Multicyclic compounds and pharmaceutical compositions comprising them are described, along with methods of their use in the treatment of diseases such as age-associated memory impairment, Alzheimer's disease, Attention-Deficit/Hyperactivity Disorder (ADD/ADHD), autism, Down syndrome, Fragile X syndrome, Huntington's disease, Parkinson's disease, and schizophrenia.Type: ApplicationFiled: March 24, 2009Publication date: July 16, 2009Inventors: Joseph Barbosa, Yingzhi Bi, Cynthia Anne Fink, Michael Alan Green, Jian Cheng Wang
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Patent number: 7504411Abstract: A pyrimidone derivative having tau protein kinase 1 inhibitory activity which is represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof; useful for prventive and/or therapeutic treatment of diseass such as neurodegenerative diseases (e.g. Alzheimer disease); wherein Q represents CH or nitrogen atom; R represents a C1-C12 alkyl group; the ring of Formula (I): represents piperazine ring or piperidine ring; each X independently represents a C1-C8 alkyl group, an optionally partially hydrogenated C6-C10 aryl ring, an indan ring or the like; m represents an integer of 1 to 3; each independently represents a halogen atom, a hydroxy group, a cyano group, a C1-C6 alkyl group or the like; n represents an integer of 0 to 8; when X and Y or two Y groups are attached on the same carbon atom, they may combine to each other to form a C2-C6 alkylene group.Type: GrantFiled: March 26, 2004Date of Patent: March 17, 2009Assignees: Mitsubishi Tanabe Pharma Corporation, Sanofi-AventisInventors: Kazutoshi Watanabe, Fumiaki Uehara, Shinsuke Hiki, Satoshi Yokoshima, Yoshihiro Usui, Masahiro Okuyama, Aya Shoda, Keiichi Aritomo, Toshiyuki Kohara, Kenji Fukunaga
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Publication number: 20090042917Abstract: A plant disease control agent contains, as an active ingredient, at least one aminopyrimidine derivatives represented by General Formula [I]: wherein R is a C2-10 alkyl group; R1 and R2 are each independently a hydrogen atom or a substituent such as an optionally substituted C1-10 alkyl group; X is hydrogen or a substituent selected from a predefined substituent group; Y is a substituent selected from a predefined substituent group; and m is an integer from 0 to 3, and agriculturally acceptable salts thereof.Type: ApplicationFiled: January 18, 2007Publication date: February 12, 2009Applicants: KUMIAI CHEMICAL INDUSTRY CO., LTD., IHARA CHEMICAL INDUSTRY CO., LTD.Inventors: Junichiro Bessho, Masao Nakatani, Yuuki Hirano, Hirokazu Arai, Atsushi Kogure, Norihisa Yonekura, Ryo Hanai
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Publication number: 20090036475Abstract: This invention relates to novel potassium channel modulating agents, and their use in the preparation of pharmaceutical compositions.Type: ApplicationFiled: March 20, 2006Publication date: February 5, 2009Applicant: NEUROSEARCH A/SInventors: Birgitte L. Eriksen, Lene Teuber, Charlotte Hougaard, Ulrik Svane Sorensen
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Patent number: 7479495Abstract: N-heterocyclic compounds that block cytokine production via inhibition of p38 kinase are disclosed. In one embodiment, compounds of the present invention are represented by Formula I: Methods of production, pharmaceutical compositions and methods of treating conditions associated with inappropriate p38 kinase activity or TNF-? expression utilizing compounds of the present invention are also disclosed.Type: GrantFiled: June 2, 2005Date of Patent: January 20, 2009Assignees: Pharmacopeia, Inc., Bristol-Myers Squibb CompanyInventors: Kevin Joseph Moriarty, Yvonne Shimshock, Gulzar Ahmed, Junjun Wu, James Wen, Wei Li, Shawn David Erickson, Jeffrey John Letourneau, Edward McDonald, Katerina Leftheris, Stephen T. Wrobleski, Zahid Hussain, Ian Henderson, Axel Metzger, John J. Baldwin, Alaric J. Dyckman
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Publication number: 20080312163Abstract: This disclosure relates generally to methods and pharmaceutical compositions useful in treating pulmonary hypertension. In one embodiment, for example, the disclosure provides a method for treating pulmonary hypertension comprising administering a therapeutically effective dose of a carbonic anhydrase inhibitor to a patient in need of treatment. The disclosure finds utility in the fields of medicine and pharmacology.Type: ApplicationFiled: June 13, 2007Publication date: December 18, 2008Inventors: Thomas Najarian, Peter Y. Tam, Leland F. Wilson, Craig Peterson
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Patent number: 7452897Abstract: The invention relates to therapeutic uses of a 2-(diaza-bicyclo-alkyl)-pyrimidone derivative represented by formula (I): Wherein R1, R2, R3, R4 and n are as defined herein. Specifically, the compounds of formula (I) are used for preventive and/or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3?, such as Alzheimer's disease. The invention relates also to intermediates for the preparation of compound of formula (I).Type: GrantFiled: March 29, 2007Date of Patent: November 18, 2008Assignees: Sanofi-Aventis, Mitsubishi Pharma CorporationInventors: Alistair Lochead, Mourad Saady, Franck Slowinski, Philippe Yaiche
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Publication number: 20080269266Abstract: There is provided novel pyrimidine derivatives of formula (I) or pharmaceutically acceptable salts thereof, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: ApplicationFiled: March 26, 2008Publication date: October 30, 2008Applicant: ASTRAZENECA ABInventors: Thorsten Nowak, Andrew Peter Thomas, Stuart Charles Purkiss
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Patent number: 7432266Abstract: Selective PDE4 inhibition is achieved by aryl and heteroaryl pyrazole compounds. The compounds exhibit improved PDE4 inhibition as compared to compounds such as rolipram and show selectivity with regard to inhibition of other classes of PDEs.Type: GrantFiled: October 14, 2005Date of Patent: October 7, 2008Assignee: Memory Pharmaceuticals CorporationInventors: Allen Hopper, Robert F. Dunn, Erik Mikal Kuester, Richard D. Conticello
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Publication number: 20080221132Abstract: The present invention relates to the compositions, methods, and applications of a novel approach to selective inhibition of several cellular or molecular targets with a single small molecule. More specifically, the present invention relates to multi-functional small molecules wherein one functionality is capable of inhibiting histone deacetylases (HDAC) and the other functionality is capable of inhibiting a different cellular or molecular pathway involved in aberrant cell proliferation, differentiation or survival.Type: ApplicationFiled: September 10, 2007Publication date: September 11, 2008Inventors: Xiong Cai, Changgeng Qian, Stephen Gould, Haixiao Zhai
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Patent number: 7405222Abstract: Disclosed are methods and compositions for treatment of male sexual dysfunction. A method of treating male sexual dysfunction includes administering a pharmaceutical composition effective to cause said male to sustain an erection. The composition is formulated based on diagnostic assessment and an individualized formulation test step. Also within the invention is a method of treating male sexual dysfunction in a population of subjects. The invention further provides kits for treatment of male erectile dysfunction.Type: GrantFiled: January 24, 2003Date of Patent: July 29, 2008Assignee: Modular Properties, Ltd.Inventors: Ramsey Sallis, Quoc Huan Ha
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Publication number: 20080146596Abstract: Multicyclic compounds, pharmaceutical compositions comprising them, and methods of their use are described.Type: ApplicationFiled: November 5, 2007Publication date: June 19, 2008Inventors: Joseph Barbosa, Yingzhi Bi, Cynthia Anne Fink, Michael Alan Green, Jian Cheng Wang
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Patent number: 7378413Abstract: A pyrimidone derivative represented by formula (I) or a salt thereof: Wherein: R1 represents a hydrogen atom or a C1-6 alkyl group which may be substituted by a C6,10 aryl group; R2 represents a C1-10 alkyl group which may be substituted, a C2-6 alkenyl group which may be substituted, a C3-6 alkynyl group which may be substituted, a C3-6 cycloalkyl group which may be substituted, or a C6-10 ARYL group which may be substituted; or R1 and R2 form together a C2-6 alkylene group which may be substituted; or R1 and R2 form together a chain of formula —(CH2)2—X—(CH2)2— or —(CH2)2—X—(CH2)3— where X represents a oxygen atom, a sulfur atom, or a nitrogen atom which may be substituted; R3 represents a 2, 3 or 4-pyridyl group optionally substituted by a C1-4 alkyl group, C1-4 alkoxy group or halogen atom; and 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.Type: GrantFiled: January 13, 2005Date of Patent: May 27, 2008Assignees: Sanofi Aventis, Mitsubishi Pharma CorporationInventors: Antonio Almario Carcia, Ryoichi Ando, Keiichi Arimoto, Fumiaki Uehara, Adrien Tak Li, Aya Shoda, Jonathan Reid Frost, Kazutoshi Watanabe
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Patent number: 7211581Abstract: The invention relates to a 2-(diaza-bicyclo-alkyl)-pyrimidone derivative represented by formula (I): wherein: R1 represents a hydrogen atom, a C1-6 alkyl group or a halogen atom; R2 represents a hydrogen atom, a C1-6 alkyl group optionally substituted by 1 to 4 substituents selected from a halogen atom, a hydroxyl group, a C1-4 alkoxy group; a C1-2 perhalogenated alkyl group, a benzyl group, a phenethyl group, a benzyloxycarbonyl group, a C1-4 alkoxy carbonyl group, a benzene ring, a naphthalene ring, a quinoline ring, a phthalazine ring, a 5,6,7,8-tetrahydronaphthalene ring, a pyridine ring, an indole ring, a pyrrole ring, a thiophene ring, a benzenesulfonyl group, a benzoyl group, a pyridazine ring, a furan ring and an imidazole ring; each of the benzyl group, the phenethyl group, the benzyloxycarbonyl group, the benzenesulfonyl group, the benzoyl group and the benzene, naphthalene, quinoline, phthalazine, 5,6,7,8-tetrehydronaphthalene, pyridine, indole, pyrrole and thiophene rings being optionally subType: GrantFiled: September 6, 2005Date of Patent: May 1, 2007Assignees: Sanofi-Aventis, Mitsubishi Pharma CorporationInventors: Alistair Lochead, Mourad Saady, Franck Slowinski, Philippe Yaiche
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Patent number: 7202251Abstract: The present invention is directed to compounds of the formula: that are antagonists of CGRP receptors and that are useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.Type: GrantFiled: March 10, 2004Date of Patent: April 10, 2007Assignee: Merck & Co., Inc.Inventors: Ian M. Bell, Steven N. Gallicchio, Cory R. Theberge, Xu-Fang Zhang, Craig Stump, C. Blair Zartman
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Patent number: 7151096Abstract: The invention provides a novel class of cyclic compounds, pharmaceutical compositions comprising such cyclic compounds and methods of using such compounds to treat or prevent diseases and disorders associated with cyclin-dependent kinases (CDKs) activity, particularly diseases associated with the activity of CDK2 and CDK5.Type: GrantFiled: March 5, 2004Date of Patent: December 19, 2006Assignee: IRM LLCInventors: Pingda Ren, Francisco Adrian, Nathanael S. Gray, Xia Wang
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Patent number: 7115601Abstract: 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.Type: GrantFiled: May 12, 2005Date of Patent: October 3, 2006Assignee: Bristol-Myers Squibb CompanyInventors: B. Narasimhulu Naidu, Margaret E. Sorenson
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Patent number: 7091201Abstract: The invention relates to novel aryl-alkane-sulfonamides 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 endothelin receptor antagonists.Type: GrantFiled: August 28, 2001Date of Patent: August 15, 2006Assignee: Actelion Pharmaceuticals Ltd.Inventors: Thomas Weller, Martin Bolli, Christoph Boss, Martine Clozel, Walter Fischli
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Patent number: 7087597Abstract: Compounds of the formula wherein R1, R2, R3, R4, X and Y are as defined, which have a superior cGMP specific phosphodiesterase (PDE) inhibitory activity, and can be used as an agent for the treatment of cardiovascular diseases such as angina pectoris, heart failure, cardiac infarction, hypertension, arteriosclerosis, and the like; allergic diseases such as asthma, or disorders of male or female genital function and the like.Type: GrantFiled: October 11, 2000Date of Patent: August 8, 2006Assignee: Takeda Pharmaceutical Company LimitedInventors: Tetsuo Miwa, Mitsuo Yamamoto, Takayuki Doi, Naoki Tarui
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Patent number: 7067523Abstract: Pests can be controlled by applying an effective amount of a compound of formula (1): wherein R is C2–C6 alkyl, C3–C6 cycloalkyl, (C3–C6 cycloalkyl)C1–C2 alkyl, 3,3,3-trifluoropropyl or 3,3,3-trifluoro-2-methylpropyl to pests or habitats of pests.Type: GrantFiled: May 21, 2003Date of Patent: June 27, 2006Assignee: Sumitomo Chemical Company, LimitedInventors: Osamu Matsumoto, Michihiko Fujinami
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Patent number: 7015228Abstract: Compounds of formula wherein R1 and R2 are each independently of the other hydrogen; unsubstituted or mono- or poly-halo-substituted C1–C20alkyl, C1–C20alkoxy, C2–C20alkenyl, C2–C20alkynyl, C3–C18cycloalkyl, C3–C7cycloalkyl-C1–C20alkyl; hydroxy; C1–C6alkoxy-C1–C20alkyl; carboxy; C1–C6alkyloxycarbonyl; cyano; mono- or di-C1–C20alkylamino; C1–C6alkylamino-C1–C20alkyl; halogen; phenyl; unsubstituted or C1–C5alkyl-, halo- or hydroxy-substituted phenyl-C1–C20alkyl, phenoxy or phenyl-C1–C20alkoxy; or R1 and R2 form a polymethylene chain of formula —(CH2)m— wherein m=2–12; R3 is unsubstituted C7–C20alkyl; or amino-, hydroxy-, carboxy- or C1–C6alkyloxycarbonyl-substituted C2–C20alkyl; C8–C18cycloalkyl; C8–C20alkenyl; C8–C20alkynyl; C3–C7cycloalkyl-C8–C20alkyl; C1–C4alkoxy-C8–C20alkyl; R7R8N—C7–C20alkyl; phenyl; phenyl-C1–C4alkyl; or phenyl-C1–C4alkoxy; R4 is hydrogen; unsubstituted or C1–C5alkyl-, halo- or hydroxy-substituted C1–C20alkyl, C2–C20alkenyl, C2–C20alkynyl, C3–C20cycloalkyl, C3–C7cycloalkyl-C1–C20alkyType: GrantFiled: April 17, 2002Date of Patent: March 21, 2006Assignee: Ciba Specialty Chemicals CorporationInventors: Wolfgang Haap, Werner Hölzl, Karin Petzold
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Patent number: 6919329Abstract: The present invention provides antibacterial agents having the formulae I, II, and III described herein.Type: GrantFiled: February 24, 2003Date of Patent: July 19, 2005Assignee: Pharmacia & Upjohn CompanyInventors: Richard Charles Thomas, Toni-Jo Poel, Michael Robert Barbachyn, Mikhail F. Gordeev, Gary W. Luehr, Adam Renslo, Upinder Singh
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Patent number: 6872729Abstract: A pyrimidinylbenzimidazole or triazinylbenzimidazole derivative represented by the general formula (I): wherein A is N or CR3, and R1, R2, R3, X, Y and n are as defined in the disclosure.Type: GrantFiled: March 10, 2003Date of Patent: March 29, 2005Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.Inventors: Masaru Shibata, Kiyoshi Kawai, Takechi Makihara, Norihisa Yonekura, Takehiro Kawashima, Junetsu Sakai, Norimichi Muramatsu
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Patent number: 6852717Abstract: Disclosed are compounds useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are processes of making such compounds.Type: GrantFiled: May 10, 2002Date of Patent: February 8, 2005Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Pier Francesco Cirillo, Daniel R. Goldberg, Abdelhakim Hammach, Neil Moss, John Robinson Regan
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Patent number: 6846829Abstract: N-Heterocyclic derivatives of the formula (I): are described herein, as well as other N-heterocycles, as inhibitors of nitric oxide synthase. Pharmaceutical compositions containing these compounds, methods of using these compounds as inhibitors of nitric oxide synthase and processes for synthesizing these compounds are also described herein.Type: GrantFiled: April 12, 2002Date of Patent: January 25, 2005Assignees: Berlex Laboratories, Inc., Pharmacopeia Drug Discovery, Inc.Inventors: Damian O. Arnaiz, John J. Baldwin, David D. Davey, James J. Devlin, Roland Ellwood Dolle, III, Shawn David Erickson, Kirk McMillan, Michael M. Morrissey, Michael H. J. Ohlmeyer, Gonghua Pan, Vidyadhar Madhav Paradkar, John Parkinson, Gary B. Phillips, Bin Ye, Zuchun Zhao
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Patent number: 6844335Abstract: A pyrimidone derivative represented by formula (I) or a salt thereof: Wherein: R1 represents a hydrogen atom or a C1-6 alkyl group which may be substituted by a C6,10 aryl group; R2 represents a C1-10 alkyl group which may be substituted, a C2-6 alkenyl group which may be substituted, a C3-6 alkynyl group which may be substituted, a C3-6 cycloalkyl group which may be substituted, or a C6-10 ARYL group which may be substituted; or R1 and R2 form together a C2-6 alkylene group which may be substituted; or R1 and R2 form together a chain of formula —(CH2)2—X—(CH2)2— or —(CH2)2—X—(CH2)3— where X represents a oxygen atom, a sulfur atom, or a nitrogen atom which may be substituted; R3 represents a 2, 3 or 4-pyridyl group optionally substituted by a C1-4 alkyl group, C1-4 alkoxy group or halogen atom; and 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.Type: GrantFiled: March 22, 2001Date of Patent: January 18, 2005Assignees: Sanofi-Synthelabo, Mitsubishi Pharma CorporationInventors: Antonio Almario Garcia, Ryoichi Ando, Keiichi Arimoto, Fumiaki Uehara, Adrien Tak Li, Aya Shoda, Jonathan Reid Frost, Kazutoshi Watanabe
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Patent number: 6818648Abstract: The present invention provides novel compounds, and pharmaceutical compositions thereof, and methods of using same in the treatment of affective disorders, anxiety, depression, post-traumatic stress disorders, eating disorders, supranuclear palsey, irritable bowl syndrome, immune supression, Alzheimer's disease, gastrointestinal diseases, anorexia nervosa, drug and alcohol withdrawal symptoms, drug addiction, inflammatory disorders, or fertility problems. The novel compounds provided by this invention are those of formula: wherein R1, R3, R5, Q, Z, Y, V, X and X′ are as defined herein.Type: GrantFiled: March 17, 2003Date of Patent: November 16, 2004Assignee: Bristol-Myers Squibb PharmaInventors: Robert John Chorvat, Parthasarathi Rajagopalan
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Patent number: 6787539Abstract: The invention relates to compounds of the formula wherein R1 is lower alkyl, lower alkoxy, pyridinyl, pyrimidinyl, phenyl, —S-lower alkyl, —S(O)2-lower alkyl, —N(R)—(CH2)n—N(R)2, —O—(CH2)n—N(R)2, —N(R)2, or a cyclic tertiary amine of the group which may contain one additional heteroatom, selected from N, O or S, and wherein this group may be connected with the pyrimidine ring via the linker —O(CH2)n—; R2 is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl; R3/R3′ is, independently from each other, hydrogen or lower alkyl; R4 is independently from each other halogen, trifluoromethyl or lower alkoxy; R5 is hydrogen or lower alkyl; R is, independently from each other, hydrogen or lower alkyl; X is —C(O)N(R)— or —N(R)C(O)—; Y is —O—, —S—, —SO2—, - or —N(R)—; n is 1,2,3 or 4; and m is 0,1 or 2; or a pharmaceuticType: GrantFiled: October 15, 2001Date of Patent: September 7, 2004Assignee: Hoffmann-La Roche Inc.Inventor: Heinz Stadler
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Patent number: 6765009Abstract: Disclosed are novel 1,4-disubstituted benzo-fused compounds wherein G, X, L, Q, n and Y are defined herein. The compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are processes of making such compounds.Type: GrantFiled: April 10, 2002Date of Patent: July 20, 2004Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Pier Francesco, Daniel R. Goldberg, Abdelhakim Hammach, Neil Moss, Kristen Mueller, John Robinson Regan
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Patent number: 6756380Abstract: Compounds of the general formula are described: wherein R1 is hydrogen or halogen; R2 is hydrogen, halogen, lower alkyl or lower alkoxy; R3 is halogen, trifluoromethyl, lower alkoxy or lower alkyl; R4/R4′are each independently hydrogen or lower alkyl; R5 is lower alkyl, lower alkoxy, amino, hydroxy, hydroxy-lower alkyl, —(CH2)n-piperazinyl, optionally substituted by lower alkyl, —(CH2)n-morpholinyl, —(CH2)n+1-imidazolyl, —O—(CH2)n+1-morpholinyl, —O—(CH2)n+1-piperidinyl, lower alkyl-sulfanyl, lower alkyl-sulfonyl, benzylamino, —NH—(CH2)n+1N(R4″)2, —(CH2)n—NH—(CH2)n+1N(R4″)2, —(CH2)n+1N(R4″)2, or —O—(CH2)n+1N(R4″)2, wherein R4″ is hydrogen or lower alkyl; R6 is hydrogen; R2 and R6 or R1 and R6 may together be —CH═CH—CH═CH—, wherein R2 and R6 or R1 and R6, respectively, together with the two carbon rinType: GrantFiled: May 22, 2000Date of Patent: June 29, 2004Assignee: Hoffmann-La Roche Inc.Inventors: Michael Bös, Guido Galley, Thierry Godel, Torsten Hoffmann, Walter Hunkeler, Patrick Schnider, Heinz Stadler
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Patent number: 6753332Abstract: The present invention relates to compounds of the formula wherein R1, R3, R5 and A are defined as in the specification, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the invention are useful in the treatment of inflammation and other inflammation associated disorders, such as osteoarthritis, rheumatoid arthritis, colon cancer and Alzheimer's disease, in mammals (preferably humans, dogs, cats and livestock).Type: GrantFiled: July 3, 2002Date of Patent: June 22, 2004Assignee: Pfizer, Inc.Inventors: Subas M. Sakya, Andrei Shavnya, Bryson Rast
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Patent number: 6716851Abstract: The present invention is directed to substituted 2-aryl-4-arylaminopyrimidine and analogs thereof, represented by the general Formula I: wherein A, Ar1, Ar2, R1 and R3 are defined herein. The present invention also relates to the discovery that compounds having Formula I are activators of caspases and inducers of apoptosis. The compounds of this invention may be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.Type: GrantFiled: December 12, 2001Date of Patent: April 6, 2004Assignee: Cytovia, Inc.Inventors: Sui Xiong Cai, John A. Drewe, Bao Nguyen, Azra Pervin
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Patent number: 6657060Abstract: Pyrimidine derivatives have been found to be useful as neuropeptide Y receptor ligands and particularly as antagonists. These pyrimidine derivatives may be used in the form of pharmaceutical preparations for the treatment or prevention of arthritis, diabetes, eating disorders, and obesity.Type: GrantFiled: November 8, 2001Date of Patent: December 2, 2003Assignee: Hoffman-La Roche Inc.Inventors: Volker Breu, Frank Dautzenberg, Patrizio Mattei, Werner Neidhart, Philippe Pflieger
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Patent number: RE41894Abstract: Racemates, diastereoisomers and optical isomers of a compound of formula (I): wherein B is H, a C6 or C10 aryl, C7-16 aralkyl; Het or (lower alkyl)-Het, all of which optionally substituted with C1-6 alkyl; C1-6 alkoxy; C1-6 alkanoyl; hydroxy; hydroxy-alkyl; halo; haloalkyl; nitro; cyano; cyanoalkyl; amino optionally substituted with C1-6 alkyl; amido; or (lower alkyl)amide; or B is an acyl derivative of formula R4—C(O)—; a carboxyl of formula R4—O—C(O)—; an amide of formula R4—N(R5)—C(O)—; a thioamide of formula R4—N(R5)—C(S)—; or a sulfonyl of formula R4—SO2; R5 is H or C1-6 alkyl; and Y is H or C1-6 alkyl; R3 is C3-7 cycloalkyl, or C4-10 alkylcycloalkyl, all optionally substituted with hydroxy, C1-6 alkoxy, C1-6 thioalkyl, amido, (lower alkyl)amido, C6 or C10 aryl, or C7-16 aralkyl; R2 is CH2—R20, NH—R20, O—R20 or S—R20, wherein R20 is a saturated or unsaturated C3-7 cycloalkyl or C4-10 (alkylcycloalkyl), all of which being optionally mono-, di- or tri-substituted with R21, or R20 is a C6 or C10 arylType: GrantFiled: March 5, 2008Date of Patent: October 26, 2010Assignee: Boehringer Ingelheim Canada Ltd.Inventors: Montse Llinas-Brunet, Murray D. Bailey, Dale R. Cameron, Elise Ghiro, Nathalie Goudreau, Marc-Andre Poupart, Jean Rancourt, Youla S. Tsantrizos, Anne-Marie Faucher, Teddy Halmos, Dominik M. Wernic