1,3-diazole Ring (including Hydrogenated) Patents (Class 544/139)
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Patent number: 7566789Abstract: Novel compounds of the formula I in which D, X, X?, W, Y, T and R1 are as defined in Patent claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic diseases and for the treatment of tumours.Type: GrantFiled: July 4, 2003Date of Patent: July 28, 2009Assignee: Merck Patent GmbHInventors: Dieter Dorsch, Bertram Cezanne, Wrner Mederski, Christos Tsaklakidis, Johannes Gleitz, Christopher Barnes
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Publication number: 20090182144Abstract: The present invention aims to provide compounds which have an inhibitory effect on the binding between S1P and its receptor Edg-1(S1P1) and which are useful for pharmaceutical purposes. A compound represented by formula (I) or a pharmaceutically acceptable salt thereof: [wherein Ar represents a monocyclic heterocyclic ring containing one or two nitrogen atoms, A represents an oxygen atom or the like, Y1, Y2 and Y3 each represent a carbon atom or a nitrogen atom, R1 represents a hydrogen atom, a C1-C6 alkyl group or the like, R2 represents a C1-C6 alkyl group, a C3-C8 cycloalkyl group or the like, R3 represents a C1-C18 alkyl group or the like, R4 represents a hydrogen atom or a C1-C6 alkyl group, and R5 represents a C1-C10 alkyl group or the like].Type: ApplicationFiled: February 6, 2007Publication date: July 16, 2009Applicant: Taisho Pharmaceutical Co., Ltd.Inventors: Naoya Ono, Tetsuo Takayama, Fumiyasu Shiozawa, Hironori Katakai, Tetsuya Yabuuchi, Tomomi Ota, Takeshi Koami, Rie Nishikawa
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Publication number: 20090181957Abstract: This invention relates to compounds of the formula (I): or pharmaceutically acceptable salts thereof, wherein: A, B, R1, R2 and R3 are each as described herein, and compositions containing such compounds and the use of such compounds in the treatment of a condition mediated by CB2 receptor binding activity such as, but not limited to, inflammatory pain, nociceptive pain, neuropathic pain, fibromyalgia, chronic low back pain, visceral pain, acute cerebral ischemia, pain, chronic pain, acute pain, post herpetic neuralgia, neuropathies, neuralgia, diabetic neuropathy, HIV-related neuropathy, nerve injury, rheumatoid arthritic pain, osteoarthritic pain, back pain, cancer pain, dental pain, fibromyalgia, neuritis, sciatica, inflammation, neurodegenerative disease, cough, broncho constriction, irritable bowel syndrome (IBS), inflammatory bowel disease (IBD), colitis, cerebrovascular ischemia, emesis such as cancer chemotherapy-induced emesis, rheumatoid arthritis, asthma, Crohn's disease, ulcerative colitis, asthmaType: ApplicationFiled: March 2, 2006Publication date: July 16, 2009Inventors: Kazuo Ando, Makoto Kawai, Tsutomu Masuda, Hirofumi Omura
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Publication number: 20090170812Abstract: Substituted benzoimidazole compounds useful as anti-infectives that decrease resistance, virulence, or growth of microbes are provided. Methods of making and using substituted benzoimidazole compounds, as well as pharmaceutical preparations thereof, in, e.g., reducing antibiotic resistance and inhibiting biofilms.Type: ApplicationFiled: June 25, 2007Publication date: July 2, 2009Applicant: Paratek Pharmaceuticals, Inc.Inventors: Michael N. Alekshun, Victoria Bartlett, Lynne Garrity-Ryan, Mark Grier, Oak K. Kim, Atul K. Verma
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Publication number: 20090163499Abstract: Compounds of the formula I: wherein R1 is optionally substituted imidazolyl, and R2, R3, R4, R5, R6, R7 and R8 are as defined herein. Also provided are methods of using the compounds for treating diseases mediated by a P2X3 and/or a P2X2/3 receptor antagonist and methods of making the subject compounds.Type: ApplicationFiled: December 17, 2008Publication date: June 25, 2009Inventors: Li Chen, Michael Patrick Dillon, Lichun Feng, Ronald Charles Hawley, Minmin Yang
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Publication number: 20090163472Abstract: The present invention provides a compound of Formula (I): or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising a compound of Formula (I) in combination with a suitable carrier, diluent, or excipient; and methods for treating physiological disorders, particularly congestive heart failure, hypertension, diabetic nephropathy, or chronic kidney disease, comprising administering a compound of Formula (I), or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: December 9, 2008Publication date: June 25, 2009Inventors: Konstantinos GAVARDINAS, Prabhakar Kondaji Jadhav
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Publication number: 20090143375Abstract: Objects of the present invention are the compounds of formula I their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, medicaments containing them and their manufacture, as well as the use of the above-mentioned compounds in the control or prevention of illnesses such as cancer.Type: ApplicationFiled: December 13, 2006Publication date: June 4, 2009Applicant: F. HOFFMANN-LA ROCHE AGInventors: Guy Georges, Bernhard Goller, Hans-Willi Krell, Anja Limberg, Ulrike Reiff, Petra Rueger, Matthias Rueth, Christine Schuell, Mark Stahl
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Publication number: 20090137584Abstract: This invention relates to compounds of the formula (I): or a pharmaceutically acceptable salt thereof, wherein A, R1, R2, R3, R4, R5, m and n are each as described herein, and compositions containing such compounds, and the use of such compounds in the treatment of a condition mediated by CB2 receptor activity such as, but not limited to, inflammatory pain, nociceptive pain, neuropathic pain, fibromyalgia, chronic low back pain, visceral pain, acute cerebral ischemia, pain, chronic pain, acute pain, post herpetic neuralgia, neuropathies, neuralgia, diabetic neuropathy, HIV-related neuropathy, nerve injury, rheumatoid arthritic pain, osteoarthritic pain, back pain, cancer pain, dental pain, fibromyalgia, neuritis, sciatica, inflammation, neurodegenerative disease, cough, broncho constriction, irritable bowel syndrome (IBS), inflammatory bowel disease (IBD), colitis, cerebrovascular ischemia, emesis such as cancer chemotherapy-induced emesis, rheumatoid arthritis, asthma, Crohn's disease, ulcerative colitis, asType: ApplicationFiled: February 23, 2007Publication date: May 28, 2009Inventors: Tomoki Kato, Kana Kon-I, Yohei Yuki, Kazuo Ando
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Publication number: 20090137585Abstract: N-Benzoyl arylsulfonamides having the formula are BCL-Xl inhibitors and are useful for promoting apoptosis. Also disclosed are BCL-Xl inhibiting compositions and methods of promoting apoptosis in a mammal.Type: ApplicationFiled: February 3, 2009Publication date: May 28, 2009Applicant: ABBOTT LABORATORIESInventors: David J. Augeri, Steven A. Baumeister, Milan Bruncko, Daniel A. Dickman, Hong Ding, Jurgen Dinges, Stephen W. Fesik, Philip J. Hajduk, Aaron R. Kunzer, William Mcclellan, David G. Nettesheim, Thorsten Oost, Andrew M. Petros, Saul H. Rosenberg, Wang Shen, Sheela A. Thomas, Xilu Wang, Michael D. Wendt
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Publication number: 20090131401Abstract: Substituted benzoimidazole compounds useful as anti-infectives that decrease resistance, virulence, or growth of microbes are provided. Methods of making and using substituted benzoimidazole compounds, as well as pharmaceutical preparations thereof, in, e.g., reducing antibiotic resistance and inhibiting biofilms.Type: ApplicationFiled: February 12, 2008Publication date: May 21, 2009Applicant: Paratek Pharmaceuticals, Inc.Inventors: Stuart B. Levy, Michael N. Alekshun, Brent L. Podlogar, Kwasi Ohemeng, Atul K. Verma, Tadeusz Warchol, Beena Bhatia, Todd Bowser, Mark Grier
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Publication number: 20090124621Abstract: The present invention provides compounds having the general structure I, or a pharmaceutically acceptable salt thereof: wherein X is a six-member ring selected from phenyl, pyridine, or pyrimidine; Y is H, an alkenyl, a substituted alkenyl, or alkynyl, and R is H or alkyl. Pharmaceutical compositions for treating various disorders such as cancers, the compositions including compound I are also provided.Type: ApplicationFiled: October 30, 2008Publication date: May 14, 2009Applicant: Burnham Institute for Medical ResearchInventor: Maurizio Pellecchia
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Publication number: 20090124615Abstract: The present invention provides benzimidazole thiophene compounds pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceutical agents.Type: ApplicationFiled: May 29, 2007Publication date: May 14, 2009Inventors: Kevin Kuntz, Kyle Allen Emmitte, Tara Renae Rheault, Stephon Smith, Keith Hornberger, Hamilton Dickson, Mui Cheung
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Publication number: 20090118200Abstract: The present invention is directed to proline bis-amide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. 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 orexin receptors are involved.Type: ApplicationFiled: May 22, 2006Publication date: May 7, 2009Inventors: Jeffrey M. Bergman, Paul J. Coleman, Christopher D. Cox, George D. Hartman, Craig Lindsley, Swati Pal Mercer, Anthony J. Roecker, David B. Whitman
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Publication number: 20090111803Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, TNF—or combinations thereof.Type: ApplicationFiled: December 18, 2008Publication date: April 30, 2009Inventors: Wensheng Yu, Ling Tong, Lei Chen, Joseph A. Kozlowski, Brian J. Lavey, Neng-Yang Shih, Vincent S. Madison, Guowei Zhou, Peter Orth, Zhuyan Guo, Michael K.C. Wong, De-Yi Yang, Seong Heon Kim, Bandarpalle B. Shankat
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Patent number: 7521448Abstract: Compounds represented by Formula (I): or a pharmaceutically acceptable salt or N-oxide thereof, are useful in the treatment of cancer.Type: GrantFiled: August 16, 2004Date of Patent: April 21, 2009Assignee: OSI Pharmaceuticals, Inc.Inventors: Joshua Bolger, Arlindo L. Castelhano, Andrew Phillip Crew, Han-Qing Dong, Ayako Honda, Radoslaw Laufer, An-Hu Li, Kristen Mulvihill, Li Qiu, Colin Peter Sambrook Smith, Yingchaun Sun, Graham Michael Wynne, Tao Zhang
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Publication number: 20090088428Abstract: The present invention discloses novel compounds of Formula I: (I) having 11?-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, and other conditions associated with 11?-HSD type 1 activity.Type: ApplicationFiled: April 19, 2007Publication date: April 2, 2009Inventors: Ashraf Saeed, Owen Brendan Wallace, Yanping Xu, Thomas Edward Mabry, Rebecca Lynn Rezac Guenther, Nancy June Snyder
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Publication number: 20090082329Abstract: The disclosure relates to compounds of formula (I): wherein Ra, Rb, R, and n are as defined in the disclosure, to pharmaceutical compositions comprising said compounds, and to processes for making and methods of using the same.Type: ApplicationFiled: July 15, 2008Publication date: March 26, 2009Applicant: AVENTIS PHARMA S.A.Inventors: Frank HALLEY, Youssef EL-AHMAD, Victor CERTAL, Corinne VENOT, Anne DAGALLIER, Hartmut STROBEL, Kurt RITTER, Sven RUF
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Publication number: 20090069322Abstract: Compounds of formula (I) are antibacterial or antiprotozoal agents for treatment of infections in humans and non-human mammals, wherein: Z represents a radical of formula —N(OH)CH(?O) or formula C(?O)NH(OH); R1 represents hydrogen, methyl or trifluoromethyl, or except when Z is a radical of formula —N(OH)CH(?O), a hydroxy, halo or amino group; R2 represents a group R10—(X)n-(ALK)m— wherein R10, ALK, X, m and n are as defined in the specification; R3 represents hydrogen, (C1-C6) alkyl or phenyl(C1-C6)alkyl-; and R5 and R6 are as defined in the specification.Type: ApplicationFiled: September 26, 2006Publication date: March 12, 2009Applicant: British Biotech Pharmaceuticals Ltd.Inventors: Paul Raymond Beckett, Steven Launchbury, Gilles Pain, Lisa Marie Pratt
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Publication number: 20090068699Abstract: An inhibitor of a glutaminyl peptide cyclotransferase, and use thereof for the treatment and/or prevention of a disease or disorder selected from the group consisting of inflammatory diseases selected from a. neurodegenerative diseases, e.g. mild cognitive impairment (MCI), Alzheimer's disease, neurodegeneration in Down Syndrome, Familial British Dementia, Familial Danish Dementia, multiple sclerosis, b. chronic and acute inflammations, e.g. rheumatoid arthritis, atherosclerosis, restenosis, pancreatitis, c. fibrosis, e.g. lung fibrosis, liver fibrosis, renal fibrosis, d. cancer, e.g. cancer/hemangioendothelioma proliferation, gastric carcinomas, e. metabolic diseases, e.g. hypertension, f. and other inflammatory diseases, e.g. neuropathic pain, graft rejection/graft failure/graft vasculopathy, HIV infections/AIDS, gestosis, tuberous sclerosis. Additionally disclosed are a respective diagnostic method, assay and kit.Type: ApplicationFiled: February 28, 2008Publication date: March 12, 2009Applicant: PROBIODRUG AGInventors: Stephan Schilling, Holger Cynis, Torsten Hoffmann, Hans-Ulrich Demuth
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Patent number: 7498354Abstract: or a pharmaceutically acceptable salt or N-oxide thereof, are useful in the treatment of tumors and cancers.Type: GrantFiled: March 30, 2006Date of Patent: March 3, 2009Assignee: OSI Pharmaceuticals, Inc.Inventors: Andrew Philip Crew, Bijoy Panicker, Han-Qing Dong
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Publication number: 20090054431Abstract: The present invention relates to novel compounds which are antagonist or inverse agonists at an opioid receptor. Such compounds are useful in the treatment of obesity and related diseases and/or conditions in mammals, particularly humans. Methods of making and using such compounds are also disclosed.Type: ApplicationFiled: October 12, 2006Publication date: February 26, 2009Inventors: Kevin Karl Barvian, Jason Daniel Speake, David John Cowan, Andrew Lamont Larkin, Jerzy Ryszard Szewczyk
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Publication number: 20090048213Abstract: The present invention provides a most suitable prodrug of a cinnamide compound. The prodrug is represented by Formula (I) wherein Ra and Rb each denote a C1-6 alkyl group or the like; Xa denotes a methoxy group or a fluorine atom; Y denotes a phosphono group or the like; and A denotes a cyclic lactam derivative.Type: ApplicationFiled: July 25, 2007Publication date: February 19, 2009Inventors: Teiji Kimura, Koki Kawano, Noritaka Kitazawa, Nobuaki Sato, Toshihiko Kaneko, Koichi Ito, Mamoru Takaishi, Ikuo Kushida
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Publication number: 20090043091Abstract: A compound of formula I: and isomers, salts, solvates, chemically protected forms, and prodrugs thereof, wherein: R1 and R2 together form, along with the nitrogen atom to which they are attached, an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; and RN1 is selected from hydrogen, an optionally substituted C1-7 alkyl group, an optionally substituted C3-20 heterocyclyl group, an optionally substituted C5-20 aryl group, an acyl group, an ester group and an amido group, and its use as a pharmaceutical.Type: ApplicationFiled: September 19, 2008Publication date: February 12, 2009Applicant: KUDOS PHARMACEUTICALS LIMITEDInventors: Graeme Cameron Murray Smith, Niall Morrison Barr Martin, Xiao-Ling Fan Cockcroft, Ian Timothy Williams Matthews, Keith Allan Menear, Laurent Jean Martin Rigoreau, Marc Geoffrey Hummersone, Roger John Griffin
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Publication number: 20090042854Abstract: The present invention is directed to certain hexahydrpyrrolidinone compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.Type: ApplicationFiled: January 19, 2007Publication date: February 12, 2009Inventors: Jianming Bao, Robert J. DeVita, Huagang Lu, Sander G. Mills, Gregori J. Morriello
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Patent number: 7482448Abstract: Novel inhibitors of cathepsin S, K, B, and L, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making.Type: GrantFiled: April 24, 2006Date of Patent: January 27, 2009Assignee: Aventis Pharmaceuticals Inc.Inventors: Sukanthini Thurairatnam, David John Aldous, Vincent Leroy, Andreas Paul Timm
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Publication number: 20090018087Abstract: The present invention relates to novel inhibitors of glutaminyl cyclase and combinations thereof for the treatment of neuronal disorders, especially Alzheimer's disease, Down Syndrome, Parkinson disease, Chorea Huntington, pathogenic psychotic conditions, schizophrenia, impaired food intake, sleep-wakefulness, impaired homeostatic regulation of energy metabolism, impaired autonomic function, impaired hormonal balance, impaired regulation, body fluids, hypertension, fever, sleep dysregulation, anorexia, anxiety related disorders including depression, seizures including epilepsy, drug withdrawal and alcoholism, neurodegenerative disorders including cognitive dysfunction and dementia.Type: ApplicationFiled: October 24, 2007Publication date: January 15, 2009Applicant: PROBIODRUG AGInventors: Stephan Schilling, Mirko Buchholz, Andre Niestroj, Ulrich Heiser, Hans-Ulrich Demuth
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Publication number: 20090012291Abstract: Substituted furo[2,3-g]indazoles for lowering intraocular pressure and treating glaucoma are disclosed.Type: ApplicationFiled: September 19, 2008Publication date: January 8, 2009Applicant: Alcon, Inc.Inventors: Anura P. Dantanarayana, Jesse Albert May
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Publication number: 20080318935Abstract: The present invention provides substituted imidazoheterocyclic compounds having the structure of formula I Also provided are pharmaceutically acceptable salts, acid salts, hydrates, solvates and stereoisomers of the compounds of formula I. The compounds are useful as modulators of cannabinoid receptors and for the prophylaxis and treatment of cannabinoid receptor-associated diseases and conditions, such as pain, inflammation and pruritis.Type: ApplicationFiled: June 20, 2008Publication date: December 25, 2008Applicant: CARA THERAPEUTICS, INC.Inventors: R. Paul Beckett, Richard Foster, Christelle Henault, Janet L. Ralbovsky, Carla M. Gauss, Gary R. Gustafson, Zhiyong Luo, Ann-Marie Campbell, Tatiana E. Shelekhin
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Publication number: 20080318951Abstract: The invention is directed to compounds having the formula: wherein: Ar, r, n, X, R2-3 and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: ApplicationFiled: June 4, 2008Publication date: December 25, 2008Inventors: Paul Allegretti, Seok-Ki Choi, Paul R. Fatheree, Roland Gendron, Ryan Hudson, Keith Jendza, Robert Murray McKinnell, Darren McMurtrie, Brooke Olson
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Publication number: 20080306064Abstract: Benzimidazole derivatives, methods of preparing the same and their pharmaceutical uses for the treatment of inflammatory diseases including COPD.Type: ApplicationFiled: July 19, 2006Publication date: December 11, 2008Inventors: Lyndon Nigel Brown, Clive McCarthy, Neil John Press, Nicolas Soldermann
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Publication number: 20080306091Abstract: The present invention provides a 2-amino-5-heteroaryl-5-phenylimidazolone compound of formula I The present invention also provides methods for the use thereof to inhibit ?-secretase (BACE) and treat ?-amyloid deposits and neurofibrillary tanglesType: ApplicationFiled: July 28, 2008Publication date: December 11, 2008Applicant: WyethInventors: Michael Sotirios Malamas, Ping Zhou, William Floyd Fobare, William Ronald Solvibile, Iwan Suwandi Gunawan, James Joseph Erdei, Yinfa Yan, Patrick Michael Andrae, Dominick Anthony Quagliato
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Derivatives of [6,7-dihydro-5-imidazo[1,2-]imidazole-3-sulfonyl]-pyrrolidine-2-carboxylic acid amide
Patent number: 7462637Abstract: Derivatives of 6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-sulfonyl]-pyrrolidine-2-carboxylic acid amide which exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease.Type: GrantFiled: October 20, 2004Date of Patent: December 9, 2008Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Terence A. Kelly, Jin Mi Kim, René Marc Lemieux, Matt Aaron Tschantz -
Publication number: 20080300247Abstract: The present invention provides benzimidazole thiophene compounds pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceutical agents.Type: ApplicationFiled: May 29, 2007Publication date: December 4, 2008Inventors: Kevin Kuntz, Kyle Allen Emmitte, Tara Renae Rheault, Stephon Smith, Keith Hornberger, Hamilton Dickson, Mui Cheung
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Publication number: 20080293718Abstract: 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: November 20, 2006Publication date: November 27, 2008Applicants: ASTRAZENECA AB, ASTEX THERAPEUTICS LIMITEDInventors: Stefan Berg, Jeremy Burrows, Gianni Chessari, Miles Stuart Congreve, Johan Hedstrom, Sven Hellberg, Katharina Hogdin, Jacob Kihlstrom, Karin Kolmodin, Johan Lindstrom, Christopher Murray, Sahil Patel
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Publication number: 20080286231Abstract: Compounds of formula (I), combinations and uses thereof for disease therapy, or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof wherein: A represents and B, R1, R2, R3, R4, R5, R6 and Z are as defined throughout the description and the claims.Type: ApplicationFiled: April 18, 2008Publication date: November 20, 2008Applicant: PROBIODRUG AGInventors: Mirko Buchholz, Ulrich Heiser, Andre J. Niestroj, Robert Sommer
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Publication number: 20080287438Abstract: The present invention provides an agent for preventing or treating neuropathy having superior action and low toxicity. This agent comprises a compound represented by the formula: wherein ring A is a 5-membered aromatic heterocycle containing 2 or more nitrogen atoms, which may further have substituent(s); B is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group; X is a divalent acyclic hydrocarbon group; Z is —O—, —S—, —NR2—, —CONR2— or —NR2CO— (R2 is a hydrogen atom or an optionally substituted alkyl group); Y is a bond or a divalent acyclic hydrocarbon group; R1 is an optionally substituted cyclic group, an optionally substituted amino group or an optionally substituted acyl group, provided that when the 5-membered aromatic heterocycle represented by ring A is imidazole, then Z should not be —O—, or a salt thereof.Type: ApplicationFiled: July 15, 2008Publication date: November 20, 2008Inventors: Yu Momose, Nozomu Sakai, Tsuyoshi Maekawa, Masatoshi Hazama, Toru Kawamura, Misayo Sera
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Publication number: 20080280769Abstract: A fragment-based strategy, involving “multicomponent reaction chemistry” (MCR), can identify novel chemotypes that disrupt the p53/MDM2 or p53/MDM4 complex employs. This approach uses high resolution structural information to delineate the region of a first protein or a ligand that is nestled within the binding pocket of a second target protein. The identified region is imported into a database containing MCR scaffolds to generate a virtual library of compounds, which subsequently are docked into the binding pocket of the target protein. Results from docking then are used to select compounds for synthesis and screening. A complementary, NMR-based methodology allows for screening the ability of compounds, selected using MCR, to disrupt the p53/MDM2 or p53/MDM4 complex.Type: ApplicationFiled: April 19, 2008Publication date: November 13, 2008Inventor: Alexander Doemling
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Publication number: 20080275233Abstract: The invention encompasses ureido substituted benzoic acid compounds, compositions comprising the compounds and methods for treating or preventing diseases associated with nonsense mutations of mRNA by administering these compounds or compositions.Type: ApplicationFiled: June 17, 2008Publication date: November 6, 2008Inventors: Richard G. Wilde, James J. Takasugi, Seongwoo Hwang, Ellen M. Welch, Guangming Chen
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Publication number: 20080269217Abstract: Provided are MC4-R binding compounds of the formula XVII: wherein L2 is a linker group, and P1, P2, P3, P4, Z1, Z2, Z3, Z4, Z5, t, s, and R are as described in the specification. Methods of using the compounds to treat MC4-R associated disorders, such as disorders associated with weight loss, are also provided.Type: ApplicationFiled: May 1, 2008Publication date: October 30, 2008Applicant: Ore Pharmaceuticals, Inc.Inventors: Tricia J. Vos, Michael E. Solomon, Christopher F. Claiborne, Martin P. Maguire, Mingshi Dai, Michael Patane, Thoma H. Marsilje
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Publication number: 20080269216Abstract: The present invention relates to novel compounds having a positive allosteric GÀBAB receptor (GDR) modulator effect, methods for the preparation of said compounds and to their use, optionally in combination with a GABAB agonist, for the inhibition of transient lower esophageal sphincter relaxations, for the treatment of gastroesophageal reflux disease, as well as for the treatment of functional gastrointestinal disorders and irritable bowel syndrome (IBS).Type: ApplicationFiled: June 20, 2005Publication date: October 30, 2008Inventors: Udo Bauer, Wayne Brailsford, Vijay Chhajlani, Bryan Egner, Ola Fjellstrom, Linda Gustafsson, Jan Mattsson, Karolina Nilsson, Thomas Olsson
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Patent number: 7442716Abstract: The invention encompasses novel compounds of Formula I or pharmaceutically acceptable salts thereof. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful to treat pain and/or inflammation from a variety of diseases or conditions, such as osteoarthritis, rheumatoid arthritis and acute or chronic pain. Methods of treating diseases or conditions mediated by the mPGES-1 enzyme and pharmaceutical compositions are also encompassed.Type: GrantFiled: November 23, 2005Date of Patent: October 28, 2008Assignee: Merck Frosst Canada Ltd.Inventors: Anh Chau, Bernard Cote, Yves Ducharme, Richard Frenette, Richard Friesen, Marc Gagnon, Andre Giroux, Evelyn Martins, Hongping Yu, Tom Wu
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Publication number: 20080261953Abstract: Compounds and compositions are provided for treatment or amelioration of one or more symptoms of ?-synuclein toxicity, ?-synuclein mediated diseases or diseases in which ?-synuclein fibrils are a symptom or cause of the disease. In one embodiment, the compounds for use in the compositions and methods are heteroaryl acylguanidines, heteroarylhydrazones, dihy-dropyridones, heteroaryl and aryl styryl ketones, and heteroarylpyrazoles.Type: ApplicationFiled: September 16, 2005Publication date: October 23, 2008Applicants: WHITEHEAD INSTITUTE FOR BIOMEDICAL RESEARCH, FOLDRX PHARMACEUTICALS, INC.Inventors: Susan L. Lindquist, Tiago Outeiro, Richard Labaudiniere
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Publication number: 20080261978Abstract: The invention provides compounds of Formula (I) and pharmaceutical compositions comprising compounds of Formula (I).Type: ApplicationFiled: March 7, 2008Publication date: October 23, 2008Inventors: Michael P. Clark, Mark A. Lockwood, Florence F. Wagner, Michael G. Natchus
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Publication number: 20080249081Abstract: Disclosed herein are benzoimidazole compounds; pharmaceutical compositions comprising a therapeutically effective amount of the same; methods of modulating the activity of an MrgX1 or an MrgX2 receptor using the same; and methods of alleviating acute, chronic and neuropathic pain in a subject using the same. Also disclosed are methods of identifying a benzoimidazole compound that modulates the activity of an MrgX1 or an MrgX2 receptor; methods of identifying a benzoimidazole compound effective for the treatment of pain.Type: ApplicationFiled: October 24, 2007Publication date: October 9, 2008Inventors: Roger Olsson, Anne Eeg Knapp, Jorgen Eskildsen
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Publication number: 20080249301Abstract: The present invention provides a process for preparing benzimidazole thiophene compounds of formula (I). Intermediates used in the process are also claimed.Type: ApplicationFiled: August 28, 2006Publication date: October 9, 2008Inventors: Keith Hornberger, Mui Cheung, Mark Andrew Pobanz, Kyle Allen Emmitte, Kevin Wayne Kuntz, Jennifer Gabriel Badiang
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Publication number: 20080234266Abstract: Compounds of the formula (I), in which R, X, X? and R2, R2?, R2?, R3?, R2?? and R7 have the meanings indicated in claim 1, are inhibitors of CHK1 CHK2 and SGK kinases and can be employed, inter alia, for the treatment of cancer.Type: ApplicationFiled: June 30, 2006Publication date: September 25, 2008Inventors: Werner Mederski, Ulrich Emde, Gerhard Barnickel, Frank Zenke, Hartmut Greiner, Frank Stieber
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Publication number: 20080227781Abstract: The present invention relates to compounds of the Formula I wherein R1, R2, R3, R4, R6, R7 and A are as defined. Compounds of the Formula I have activity inhibiting production of A?-peptide. The invention also relates to pharmaceutical compositions and methods for treating diseases and disorders, for example, neurodegenerative and/or neurological disorders, e.g., Alzheimer's disease, in a mammal comprising compounds of the Formula I.Type: ApplicationFiled: January 9, 2008Publication date: September 18, 2008Inventors: Michael A. Brodney, Karen J. Coffman
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Publication number: 20080221086Abstract: The present invention relates to compounds of formula (I), combinations and uses thereof for disease therapy, or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof wherein R1 represents heteroaryl; -carbocyclyl-heteroaryl; -alkenylheteroaryl or -alkylheteroaryl; R2 represents alkyl which may optionally be substituted by hydroxy; carbocyclyl, which may optionally be substituted by one or more groups selected from alkyl and hydroxy; aryl; -aryl-heteroaryl; -heteroaryl-aryl; -aryl-heterocyclyl; H; heteroaryl; or heterocyclyl, which may optionally be substituted by one or more groups selected from alkyl oxo and hydroxy; R3 represents alkyl which may optionally be substituted by one of more groups selected from alkoxy, amine, hydroxy and —C(O)Oalkyl; carbocyclyl, which may optionally be substituted by one or more groups selected from alkyl haloalkyl, alkoxy, amine, hydroxy and —C(O)Oalkyl; -alkyl-aryl; -alkyl(aryl)2; -alkyl-heteroaryl; -alkyl(heType: ApplicationFiled: November 8, 2007Publication date: September 11, 2008Applicant: PROBIODRUG AGInventors: Michael Thormann, Michael Altmstetter, Andreas Treml, Ulrich Heiser, Mirko Buchholz, Andre J. Niestroj
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Publication number: 20080207612Abstract: Compounds of Formula (I) or pharmaceutically acceptable salts thereof; wherein R1, R2, R3, and R4 are as defined in the specification as well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.Type: ApplicationFiled: September 24, 2004Publication date: August 28, 2008Applicant: AstraZeneca ABInventors: Ziping Liu, Daniel Page, Christopher Walpole, Hua Yang
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Publication number: 20080146523Abstract: The invention relates to imidazole derivatives which have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1. The invention also relates to a pharmaceutically-suitable acid-addition salt of the above compound. The invention further relates to a composition comprising an imidazole derivative as described above, or a pharmaceutically-suitable acid-addition salt thereof, and to processes for preparing such compounds.Type: ApplicationFiled: December 5, 2007Publication date: June 19, 2008Inventors: Guido Galley, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder