Polycyclo Ring System Having The Diazole Ring As One Of The Cyclos Patents (Class 514/405)
-
Publication number: 20090149443Abstract: Compounds of formula (I): in which A, B, X, Ar1, R8 and R4 have any of the meanings given in the specification, are inhibitors of p38 useful in the treatment and prevention of various disorders mediated by p38.Type: ApplicationFiled: March 27, 2007Publication date: June 11, 2009Inventors: Mark C. Munson, Kevin W. Hunt, Christopher T. Clark, Ganghyeok Kim, Laurence E. Burgess, James P. Rizzi
-
Patent number: 7541376Abstract: The present invention provides a novel 1H-indazole compound having an excellent JNK inhibitory action. More specifically, it provides a compound represented by the following formula, a salt thereof or a hydrate of them. Wherein R1 is a C6-C14 aromatic cyclic hydrocarbon group etc.; R2, R4 and R5 each independently represent a hydrogen atom, a halogen atom, a cyano group etc.; L is a single bond, or a C1-C6 alkylene group etc.; X is a single bond, or a group represented by —CO—NH— or —NH—CO—, etc.; and Y is a C3-C8 cycloalkyl group, a C6-C14 aromatic cyclic hydrocarbon group or a 5- to 14-membered aromatic heterocyclic group etc.Type: GrantFiled: August 12, 2005Date of Patent: June 2, 2009Assignee: Eisai R&D Management Co., Ltd.Inventors: Hitoshi Oinuma, Norihito Ohi, Nobuaki Sato, Motohiro Soejima, Hidenori Seshimo, Taro Terauchi, Takashi Doko, Naohiro Kohmura
-
Patent number: 7524842Abstract: 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, aggrecanase, TNF-? or combinations thereof.Type: GrantFiled: January 16, 2007Date of Patent: April 28, 2009Assignee: Schering CorporationInventors: Brian J. Lavey, Joseph A. Kozlowski, Guowei Zhou, Ling Tong, Wensheng Yu, Michael K. C. Wong, Bandarpalle B. Shankar, Neng-Yang Shih, M. Arshad Siddiqui, Kristin E. Rosner, Chaoyang Dai, Janeta Popovici-Muller, Vinay M. Girijavallabhan, Dansu Li, Razia Rizvi, Lei Chen, De-Yi Yang, Robert Feltz, Seong Heon Kim
-
Patent number: 7517901Abstract: Compounds of formula Ia or Ib: wherein X and Y are nitrogen or CRe, and R1, R2, R3, R4 and R5 are as defined herein. Also disclosed are methods of making the subject compounds and methods of using the compounds for treatment of p38-mediated diseases.Type: GrantFiled: August 23, 2006Date of Patent: April 14, 2009Assignee: Roche Palo Alto LLCInventors: Tobias Gabriel, Michael Soth
-
Patent number: 7514463Abstract: Novel compounds useful for inhibiting spermatogenesis and cancer treatment, and in particular as inhibitors of heat shock proteins and/or elongation factor 1 alpha.Type: GrantFiled: August 20, 2004Date of Patent: April 7, 2009Assignees: University of Kansas, University of Kansas Medical CenterInventors: Gunda I. Georg, Joseph S. Tash, Ramappa Chakrasali, Sudhakar Rao Jakkaraj
-
Patent number: 7511039Abstract: There are disclosed ?-sheet mimetics and methods relating to the same for imparting or stabilizing the ?-sheet structure of a peptide, protein or molecule. In one aspect, ?-sheet mimetics are disclosed having utility as protease inhibitors in general and, more specifically, as serine protease inhibitors such as thrombin, elastase and Factor X inhibitors. In one embodiment, the ?-sheet mimetic is a thrombin inhibitor.Type: GrantFiled: June 7, 2006Date of Patent: March 31, 2009Assignee: Myriad Genetics, Inc.Inventors: Michael Kahn, Cyprian O. Ogbu, Masakatsu Eguchi, Hwa-Ok Kim, Patrick D. Boatman, Jr.
-
Patent number: 7504424Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate, ester or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF- or combinations thereof.Type: GrantFiled: January 17, 2006Date of Patent: March 17, 2009Assignee: Schering CorporationInventors: 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. Shankar, M. Arshad Siddiqui, Kristin E. Rosner, Chaoyang Dai, Umar Faruk Mansoor, Janeta Popovici-Muller, Vinay M. Girijavallabhan, Dansu Li
-
Publication number: 20090068197Abstract: Methods for detecting and treating Mycobacterium-related diseases including reducing Mycobacterial virulence, reducing RV3133c dimerization, and treating a subject with a Mycobacterial infection using identified compounds are disclosed. Examples of compounds useful in the treatment of Mycobacterium-related diseases include N-(4-[(acetylamino)sulfonyl]phenyl)-3-phenylpropanamide; 1-(3,5-di-tert-butyl-4-hydroxyphenyl)-2-(2-imino-3-methyl-2,3-dihydro-1H-benzimidazol-1yl)ethanone hydrochloride; and 1-(1,3-benzoxazol-2-yl)-3-({4-[(2-hydroxyethyl)sulfonyl]phenyl}amino)acrylaldehyde. Further disclosed are methods for identifying agents that interact with a polypeptide in a Mycobacterium cell.Type: ApplicationFiled: March 1, 2007Publication date: March 12, 2009Applicant: THE UAB RESEARCH FOUNDATIONInventors: Andries J.C. Steyn, Deborah Mai, Amit Singh
-
Publication number: 20090048250Abstract: The present invention provides compounds of formula I: These compounds, and pharmaceutically acceptable compositions thereof, are useful generally as kinase inhibitors, particularly as inhibitors of PRAK, GSK3, ERK2, CDK2, MK2, SRC, SYK, and Aurora-2. Accordingly, compounds and compositions of the invention are useful for treating or lessening the severity of a variety of disorders, including, but not limited to, heart disease, diabetes, Alzheimer's disease, immunodeficiency disorders, inflammatory diseases, allergic diseases, autoimmune diseases, destructive bone disorders such as osteoporosis, proliferative disorders, infectious diseases and viral diseases.Type: ApplicationFiled: August 20, 2007Publication date: February 19, 2009Inventors: Alex Aronov, David J. Lauffer, Huan Qiu Li, Ronald Charles Tomlinson, Pan Li
-
Publication number: 20090036508Abstract: Compounds of the formula I in which X, Y, R1, R2, R3 and R4 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: January 10, 2007Publication date: February 5, 2009Inventors: Markus Klein, Rolf Gericke, Werner Mederski, Norbert Beier, Florian Lang
-
Patent number: 7482370Abstract: 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: GrantFiled: July 13, 2005Date of Patent: January 27, 2009Assignee: Schering CorporationInventors: 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. Shankar
-
Patent number: 7473701Abstract: Substituted indazoles, compositions containing them, method of production and use. The present invention relates in particular to novel specific substituted indazoles exhibiting kinase-inhibiting activity, having therapeutic activity, in particular in oncology.Type: GrantFiled: October 13, 2004Date of Patent: January 6, 2009Assignee: Aventis Pharma S.A.Inventors: Dominique Damour, Jean-Christophe Carry, Patrick Nemecek, Corinne Terrier, Frederico Nardi, Bruno Filoche-Romme, Marie-Pierre Cherrier, Daniel Bezard
-
Publication number: 20080287516Abstract: The present invention relates to phenyl-substituted pyrrolidones and compounds related to phenyl-substituted pyrrolidones. One use of these compounds is for the inhibition of viruses, e.g., HIV. The invention further relates to methods of malting these compounds, methods of identifying the efficacy of these compounds, and methods of using these compounds to inhibit or prevent HIV infection and related disease states such as AIDS.Type: ApplicationFiled: January 30, 2006Publication date: November 20, 2008Applicant: IRM LLCInventors: Baogen Wu, Truc Ngoc Nguyen, David Archer Ellis, Xiaohui He, Beth Marie Anaclerio, Kunyong Yang, Ha-soon Choi, Zhicheng Wang, Thomas H. Marsilje, Yun He
-
Patent number: 7449585Abstract: Compounds of formula (I), which are useful as therapeutic compounds, particularly in the treatment of pain and other conditions ameliorated by the modulation of the function of the vanilloid-1 receptor (VR1).Type: GrantFiled: November 12, 2004Date of Patent: November 11, 2008Assignee: Merck Sharp & Dohme Ltd.Inventors: Frank Burkamp, Stephen Robert Fletcher
-
Patent number: 7449488Abstract: In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of protein and/or checkpoint kinases, methods of preparing such compounds, pharmaceutical compositions including one or more such compounds, methods of preparing pharmaceutical formulations including one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the protein or checkpoint kinases using such compounds or pharmaceutical compositions. The invention also relates to the inhibition of hepatitis C virus (HCV) replication. In particular, embodiments of the invention provide compounds and methods for inhibiting HCV RNA-dependent RNA polymerase enzymatic activity. The invention also provides compositions and methods for the prophylaxis and treatment of HCV infection.Type: GrantFiled: October 6, 2005Date of Patent: November 11, 2008Assignee: Schering CorporationInventors: Kamil Paruch, Timothy J. Guzi, Michael P. Dwyer, Gerald W. Shipps, Jr.
-
Publication number: 20080261997Abstract: The present invention relates to the use of novel derivatives of general formula (I) in which R3 is a (1-6C)alkyl, aryl, aryl(1-6C)alkyl, heteroaryl, heteroaryl(1-6C)alkyl, aryl or heteroaryl fused to a (1-10C) cycloalkyl, heterocycle, heterocycloalkyl, cycloalkyl, adamantyl, polycycloalkyl, alkenyl, alkynyl, CONR1R2, COOR1, SO2R1, C(?NH)R1 or C(?NH)NR1 radical; R5, R6 and R7 are, independently of one another, chosen from the following radicals: halogen, CN, NO2, NH2, OH, OR8, COOH, C(O)OR8, —O—C(O)R8, NR8R9, NHC(O)R8, C(O)NR8R9, NHC(S)R8, C(S)NR8R9, SR8, S(O)R8, SO2R8, NHSO2R8, SO2NR8R9, —O—SO2R8, —SO2—O—R8, trifluoromethyl, trifluoromethoxy, (1-6C)alkyl, (1-6C)alkoxy, aryl, aryl(1-6C)alkyl, heteroaryl, heteroaryl(1-6C)alkyl, heterocycle, cycloalkyl, alkenyl, alkynyl, adamantyl or polycycloalkyl, to treat a disease selected from the group consisting of: neurodegenerative diseases, strokes, cranial and spinal traumas and peripheral neuropathies, obesity, metabolic diseases, type II diabetes, essential hType: ApplicationFiled: June 20, 2008Publication date: October 23, 2008Applicant: AVENTIS PHARMA S.A.Inventors: Dominique LESUISSE, Gilles DUTRUC-ROSSET, Franck HALLEY, Didier BABIN, Thomas ROONEY, Gilles TIRABOSCHI
-
Publication number: 20080234348Abstract: Novel squaric acid compounds of the formula (I), in which R1, R2, R2?, R2? and X have the meanings indicated in claim 1, are inhibitors of CHK1 CHK2 and SGK kinases and can be used for the treatment of diseases and complaints such as cancer, diabetes, obesity, metabolic syndrome (dyslipidaemia), systemic and pulmonary hypertonia, cardiovascular diseases and renal diseases, generally in fibroses and inflammatory processes of any type.Type: ApplicationFiled: August 2, 2006Publication date: September 25, 2008Inventors: Werner Mederski, Rolf Gericke, Markus Klein, Norbert Beier, Florian Lang
-
Publication number: 20080234347Abstract: The present invention is directed to a method for treating, ameliorating or preventing CB2 receptor mediated pain in a subject in need thereof comprising administering to the subject an effective amount of a compound of formula (I): or a form thereof, wherein X1R1, X2R2, X3R3, X4R4 and X5R5 are as defined herein.Type: ApplicationFiled: February 27, 2008Publication date: September 25, 2008Inventors: Mingde Xia, Mark J. Macielag, Christopher M. Flores, Kevin Paul Pavlick
-
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
-
Patent number: 7425572Abstract: Novel dioxinoindazole compounds and dioxoloindazole compounds are disclosed. Also disclosed are methods for the lowering and controlling of normal or elevated intraocular pressure as well as a method for the treatment of glaucoma using compositions of one or more of the compounds of the present invention.Type: GrantFiled: December 2, 2005Date of Patent: September 16, 2008Assignee: Alcon, Inc.Inventors: Hwang-Hsing Chen, Jesse A. May
-
Publication number: 20080214641Abstract: Compounds of formula (I): The present invention relates to novel indazolyl ester or amide derivatives, to pharmaceutical compositions comprising such derivatives, to processes for preparing such novel derivatives and to the use of such derivatives as medicamentsType: ApplicationFiled: December 20, 2007Publication date: September 4, 2008Inventors: Markus Berger, Jan Dahmen, Karl Edman, Anders Eriksson, Balint Gabos, Thomas Hansson, Martin Hemmerling, Krister Henriksson, Svetlana Ivanova, Matti Lepisto, Darren McKerrecher, Magnus Munck af Rosenschold, Stinabritt Nilsson, Hartmut Rehwinkel, Camilla Taflin
-
Patent number: 7407950Abstract: The invention concerns compounds of general formula (I), wherein n, X1, X2, X3, X4, Z1, Z2, Z3, Z4, Z5 and W are as defined herein. Said compounds are ligands of the TRPV1 vanilloid receptor, and are therefore, useful for treating diseases associated with TRPV1 receptors, such as pain and inflammation.Type: GrantFiled: June 20, 2007Date of Patent: August 5, 2008Assignee: Sanofi-AventisInventors: Laurent Dubois, Yannick Evanno, Andre Malanda
-
Patent number: 7390797Abstract: The present invention provides a novel fused indazole compound having an excellent JNK inhibitory action. More specifically, it provides a compound represented by the following formula, a salt thereof or a hydrate of them. Wherein Z11 and Z12 each independently represent a carbonyl group, a methylene group, etc.; represents a double bond or a single bond; R1a represents a hydrogen atom, etc.; the ring A represents a benzene ring, a naphthalene ring or a 5- to 10-membered aromatic heterocyclic ring, etc.; and R2a, R2b and R2c each independently represent (1) a hydrogen atom, (2) a halogen atom, (3) a nitro group, etc.Type: GrantFiled: February 21, 2003Date of Patent: June 24, 2008Assignee: Eisai Co., Ltd.Inventors: Norihito Ohi, Nobuaki Sato, Naohiro Kohmura
-
Patent number: 7354944Abstract: The invention relates to thiadiazole compounds useful for treating diseases mediated by protein kinase B (PKB). The invention also relates to the therapeutic use of such thiadiazole compounds and compositions thereof in treating disease states associated with abnormal cell growth, cancer, inflammation, and metabolic disorders.Type: GrantFiled: October 18, 2005Date of Patent: April 8, 2008Assignee: Amgen Inc.Inventors: Qingping Zeng, Guomin Yao, George Erich Wohlhieter, Vellarkad N. Viswanadhan, Andrew Tasker, James Thomas Rider, Holger Monenschein, Celia Dominguez, Matthew Paul Bourbeau
-
Patent number: 7312239Abstract: An object of the present invention is to provide a medicament and method which is useful for prevention and/or therapy of arterial wall injury.Type: GrantFiled: August 18, 2003Date of Patent: December 25, 2007Assignee: Mitsubishi Pharma CorporationInventors: Takayuki Tanaka, Tatsuhiko Mori
-
Patent number: 7300950Abstract: The present invention relates to pyrazole derivatives of the formula I, their preparation and their use in pharmaceuticals: in which X, R1, R1a, R2, R3, R4 and n are as defined in the claims, which are useful pharmaceutically active compounds for the therapy and prophylaxis of illnesses, for example of cardiovascular diseases such as hypertension, angina pectoris, cardiac insufficiency, thromboses or atherosclerosis. The compounds of the formula I are capable of modulating the body's production of cyclic guanosine monophosphate “cGMP” and are generally suitable for the therapy and prophylaxis of illnesses which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of the formula I, to their use for the therapy and prophylaxis of the abovementioned illnesses and for preparing pharmaceuticals for this purpose, and also to pharmaceutical preparations which comprise the compounds of the formula I.Type: GrantFiled: April 13, 2005Date of Patent: November 27, 2007Assignee: Aventis Pharma Deutschland GmbHInventors: Ursula Schindler, Karl Schönafinger, Hartmut Strobel
-
Patent number: 7291612Abstract: The present invention relates to novel heterocyclic compounds, to methods for their preparation, to compositions containing them, and to methods and use for clinical treatment of medical conditions which may benefit from immunomodulation, including rheumatoid arthritis, multiple sclerosis, diabetes, asthma, transplantation, systemic lupus erythematosis and psoriasis. More particularly the present invention relates to novel heterocyclic compounds, which are CD80 antagonists capable of inhibiting the interactions between CD80 and CD28.Type: GrantFiled: May 30, 2006Date of Patent: November 6, 2007Assignee: Active Biotech A.B.Inventors: Ian Richard Matthews, Thomas Stephen Coutler, Chiara Ghiron, Chris James Brennan, Muhammed Kamal Uddin, Lars Olof Goran Pettersson, Dorthe da Graca Thrige, Philip Huxley
-
Patent number: 7262200Abstract: The present invention provides compounds of formula I: These compounds, and pharmaceutically acceptable compositions thereof, are useful generally as kinase inhibitors, particularly as inhibitors of PRAK, GSK3, ERK2, CDK2, MK2, SRC, SYK, and Aurora-2. Accordingly, compounds and compositions of the invention are useful for treating or lessening the severity of a variety of disorders, including, but not limited to, heart disease, diabetes, Alzheimer's disease, immunodeficiency disorders, inflammatory diseases, allergic diseases, autoimmune diseases, destructive bone disorders such as osteoporosis, proliferative disorders, infectious diseases and viral diseases.Type: GrantFiled: October 27, 2003Date of Patent: August 28, 2007Assignee: Vertex Pharmaceuticals IncorporatedInventors: Alex Aronov, David J. Lauffer, Huan Qui Li, Ronald Charles Tomlinson, Pan Li
-
Patent number: 7259183Abstract: The present invention relates to compounds of formula (I): wherein —X—Y—, R1 to R11 and n are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are mediated by CETP inhibitors.Type: GrantFiled: August 4, 2005Date of Patent: August 21, 2007Assignee: Hoffmann-La Roche Inc.Inventors: Aurelia Conte-Mayweg, Holger Kuehne, Thomas Luebbers, Cyrille Maugeais, Werner Mueller, Philippe Pflieger
-
Patent number: 7241792Abstract: The present invention relates to certain fused pyrazole derivatives of Formula (Ia), and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists for the RUP25 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, insulin resistance, type 2 diabetes, Syndrome-X and the like.Type: GrantFiled: December 22, 2005Date of Patent: July 10, 2007Assignee: Arena Pharmaceuticals, Inc.Inventors: P. Douglas Boatman, Thomas O. Schrader, Graeme Semple, Philip J. Skinner, Jae-Kyu Jung
-
Patent number: 7214699Abstract: This invention relates to compounds which are generally CRF-1 receptor antagonists and which are represented by Formula I or Formula II: wherein R3 is optionally substituted aryl or heteroaryl, R1 and R2 are as defined in the specification; or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts thereof. The invention further relates to processes for preparing such compounds, to pharmaceutical compositions containing such compounds, and to methods for their use as therapeutic agents.Type: GrantFiled: December 1, 2003Date of Patent: May 8, 2007Assignee: Roche Palo Alto LLCInventors: Richard Leo Cournoyer, David Garrett Loughhead, Counde O'Yang
-
Patent number: 7199147Abstract: A compound represented by the formula (1): wherein R1—X— indicates that 1 to 4 R1—X— groups are present which may be the same or different, the ring A is a saturated or unsaturated 5-membered heterocyclic ring, X is a single bond, a group represented by the formula: —N(R3)—, —O— or —S—, or the like. R1 is a hydrogen atom, a halogen atom, a nitro group, a carboxyl group, a substituted or unsubstituted alkyl group, or the like, R2 is a hydrogen atom, a halogen atom, a nitro group, a carboxyl group, a substituted or unsubstituted alkyl group, or the like, and R3 is a hydrogen atom, a substituted or unsubstituted alkyl group, or the like; a prodrug of said compound, or a pharmaceutically acceptable salt of said compound or prodrug is a useful compound as a therapeutic agent for diseases for which Rho kinase is responsible.Type: GrantFiled: June 6, 2002Date of Patent: April 3, 2007Assignee: Dainippon Sumitomo Pharma Co., Ltd.Inventors: Naonori Imazaki, Masafumi Kitano, Naohito Ohashi, Kazuki Matsui
-
Patent number: 7196111Abstract: The invention relates to the inhibition of hepatitis C virus (HCV) replication. In particular, embodiments of the invention provide compounds and methods for inhibiting HCV RNA-dependent RNA polymerase enzymatic activity. The invention also provides compositions and methods for the prophylaxis and treatment of HCV infection.Type: GrantFiled: June 2, 2003Date of Patent: March 27, 2007Assignee: Schering CorporationInventors: Gerald W. Shipps, Kristin E. Rosner, Janet Popovici-Muller, Yongqi Deng, Tong Wang, Patrick J. Curran
-
Patent number: 7196110Abstract: The invention is directed to N-substituted tricyclic 3-AMINOPYRAZOLE derivatives, which are useful as inhibitors of platelet-derived growth factor receptor (PDGF-R) kinase, and methods for the preparation of said derivatives. The present invention is further directed to pharmaceutical compositions comprising the compounds of the present invention and to methods for treating conditions such as tumors and other cell proliferative disorders.Type: GrantFiled: May 14, 2003Date of Patent: March 27, 2007Assignee: Janssen Phamaceutica N.V.Inventors: Chih Yung Ho, Bengt Anders Brunmark, Stuart Emanuel, Robert A. Galemmo, Jr., Dana L. Johnson, Donald W. Ludovici, Umar Maharoof, Jay M. Mei, Jan L. Sechler, Eric D. Strobel, Robert W. Tuman, Hwa Kwo Yen
-
Patent number: 7166629Abstract: The present invention relates to novel derivatives of general formula (I) in which R3 is a (1–6C)alkyl, aryl, aryl(1–6C)alkyl, heteroaryl, heteroaryl(1–6C)alkyl, aryl or heteroaryl fused to a (1–10C)cycloalkyl, heterocycle, heterocycloalkyl, cycloalkyl, adamantyl, polycycloalkyl, alkenyl, alkynyl, CONR1R2, COOR1, SO2R1, C(?NH)R1 or C(?NH)NR1 radical; R5 and R6 are, independently of one another, chosen from the following radicals: halogen, CN, NO2, NH2, OH, COOH, C(O)OR8, —O—C(O)R8, NR8R9, NHC(O)R8, C(O)NR8R9, NHC(S)R8, C(S)NR8R9, SR8, S(O)R8, SO2R8, NHSO2R8, SO2NR8R9, —O—SO2R8, —SO2—O—R8, trifluoromethyl, trifluoromethoxy, (1–6C)alkyl, (1–6C)alkoxy, aryl, aryl(1–6C)alkyl, heteroaryl, heteroaryl(1–6C)alkyl, heterocycle, cycloalkyl, alkenyl, alkynyl, adamantyl or polycycloalkyl.Type: GrantFiled: September 4, 2003Date of Patent: January 23, 2007Assignee: Aventis Pharma S.A.Inventors: Dominique Lesuisse, Gilles Dutruc-Rosset, Franck Halley, Didier Babin, Thomas Rooney
-
Patent number: 7160916Abstract: This invention features a method for enhancing bone growth or inhibiting bone resportion. The method includes administering to a subject in need thereof a compound of the following formula: A is H, R, or each of Ar1, Ar2, and Ar3, independently, is phenyl, thienyl, furyl, or pyrrolyl; each of R1, R2, R3, R4, R5, and R6, independently, is H, halogen, R, C(O)OH, C(O)OR, C(O)SH, C(O)SR, C(O)NH2, C(O)NHR, C(O)NRR?, ROH, ROR?, RSH, RSR?, NHR, NRR?, RNHR?, or RNR?R?; or R1 and R2 together, R3 and R4 together, or R5 and R6 together are ORO; wherein each of R, R?, and R?, independently is C1˜C6 alkyl; and n is 1, 2, or 3.Type: GrantFiled: September 1, 2004Date of Patent: January 9, 2007Assignee: Yung Shin Pharmaceutical Ind. Co., Ltd.Inventors: Wen-Mei Fu, Chih-Hsin Tang, Rong-Sen Yang, Che-Ming Teng, Sheng-Chu Kuo, Fang-Yu Lee
-
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
-
Patent number: 7125872Abstract: There are disclosed ?-sheet mimetics and methods relating to the same for imparting or stabilizing the ?-sheet structure of a peptide, protein or molecule. In one aspect, ?-sheet mimetics are disclosed having utility as protease inhibitors in general and, more specifically, as serine protease inhibitors such as thrombin, elastase and Factor X inhibitors. In one embodiment, the ?-sheet mimetic is a thrombin inhibitor.Type: GrantFiled: December 22, 2003Date of Patent: October 24, 2006Assignee: Myriad Genetics, Inc.Inventors: Michael Kahn, Cyprian O. Ogbu, Masakatsu Eguchi, Hwa-Ok Kim, Patrick Douglas Boatman, Jr.
-
Patent number: 7119115Abstract: The present invention relates to novel compounds derived from indazoles or indoles of formula (1) or formula (2), to methods for treating tumors or cancerous cells with compounds of formula (1) or formula (2) and to pharmacaetutical compositions comprising a pharmaceutically acceptable carrier and a compound of formula (1) or formula (2)Type: GrantFiled: January 21, 2004Date of Patent: October 10, 2006Assignee: Aventis Pharma S.A.Inventors: Michel Tabart, Eric Bacqué, Sylvie Wentzler, Cécile Combeau, Conception Nemecek, Patrick Mailliet, Fabienne Thompson
-
Patent number: 7115658Abstract: Compounds of formula I are hepatitis C virus (HCV) RNA-dependent RNA polymerase (RdRp) inhibitors, and are useful in therapeutic and prophylactic treatment of persons infected with hepatitis C virusType: GrantFiled: May 9, 2003Date of Patent: October 3, 2006Assignee: Agouron Pharmaceuticals, Inc.Inventors: Allen J. Borchardt, Peter Scott Dragovich, Javier Gonzalez, Tanya Michelle Jewell, Hui Li, Maria Angelica Linton, John Howard Tatlock, Ru Zhou, Thomas Jay Prins, Melwyn A. Abreo
-
Patent number: 7087626Abstract: Novel pyrrazole derivative compounds and their use as pharmaceutical agents, in particular their use as TGF-beta signal transduction inhibitors.Type: GrantFiled: May 13, 2002Date of Patent: August 8, 2006Assignee: Eli Lilly and CompanyInventors: Douglas Wade Beight, Todd Vincent DeCollo, Alexander Glenn Godfrey, Theodore Goodson, Jr., Hong-Yu Li, William Thomas McMillen, Shawn Christopher Miller, Jason Scott Sawyer, Edward C. R. Smith, Jonathan Michael Yingling
-
Patent number: 7081456Abstract: The present invention relates to novel heterocyclic compounds, to methods for their preparation, to compositions containing them, and to methods and use for clinical treatment of medical conditions which may benefit from immunomodulation, including rheumatoid arthritis, multiple sclerosis, diabetes, asthma, transplantation, systemic lupus erythematosis and psoriasis. More particularly the present invention relates to novel heterocyclic compounds, which are CD80 antagonists capable of inhibiting the interactions between CD80 and CD28.Type: GrantFiled: November 21, 2003Date of Patent: July 25, 2006Assignee: Active Biotech ABInventors: Ian Richard Matthews, Thomas Stephen Coulter, Chiara Ghiron, Chris James Brennan, Muhammed Kamal Uddin, Lars Olof Göran Pettersson, Dorthe da Graca Thrige, Philip Huxley
-
Patent number: 7078425Abstract: Disclosed are compounds of the Formula (I) and pharmaceutically acceptable salts and prodrugs thereof, wherein A, B, R1, R2, R3, and R4 are as defined in the specification. Such compounds are tyrosine phosphatase inhibitors and useful in the treatment or prevention of Type II Diabetes Mellitus.Type: GrantFiled: April 30, 2003Date of Patent: July 18, 2006Assignee: Array Biopharma Inc.Inventors: Robert D. Groneberg, David A. Mareska
-
Patent number: 7049334Abstract: A method for enhancing learning and memory or treating amnesia. The method includes administrating to a subject in need thereof a compound of the formula (I): A is H, R, or ?each of Ar1, Ar2, and Ar3, independently, is phenyl, thienyl, furyl, or pyrrolyl; each of R1, R2, R3, R4, R5, and R6, independently, is H, nitro, halogen, R, OH, OR, C(O)OH, C(O)OR, C(O)SH, C(O)SR, C(O)NH2, C(O)NHR, C(O)NRR?, ROH, ROR?, RSH, RSR?, ROC(O)R?OH, NHR, NRR?, RNHR?, or RNR?R?; or R1 and R2 together, R3 and R4 together, or R5 and R6 together are ORO; wherein each of R, R?, and R?, independently is C1˜C6 alkyl; and n is 1, 2, or 3. The compound is in an effective amount for enhancing learning and memory or treating amnesia.Type: GrantFiled: September 13, 2002Date of Patent: May 23, 2006Assignee: Carlsbad Technology, Inc.Inventors: Wen-Mei Fu, Keng-Chen Liang, Wei-Lin Chien, Sheng-Chu Kuo, Fang-Yuan Lee, Che-Ming Teng
-
Patent number: 7019011Abstract: The present invention relates to novel derivatives of general formula (I) in which R3 is a (1–6C)alkyl, aryl, aryl(1–6C)alkyl, heteroaryl, heteroaryl(1–6C)alkyl, aryl or heteroaryl fused to a (1–10C) cycloalkyl, heterocycle, heterocycloalkyl, cycloalkyl, adamantyl, polycycloalkyl, alkenyl, alkynyl, CONR1R2, COOR1, SO2R1, C(?NH)R1 or C(?NH)NR1 radical; R5, R6 and R7 are, independently of one another, chosen from the following radicals: halogen, CN, NO2, NH2, OH, OR8, COOH, C(O)OR8, —O—C(O)R8, NR8R9, NHC(O)R8, C(O)NR8R9, NHC(S)R8, C(S)NR8R9, SR8, S(O)R8, SO2R8, NHSO2R8, SO2NR8R9, —O—SO2R8, —SO2—O—R8, trifluoromethyl, trifluoromethoxy, (1–6C)alkyl, (1–6C)alkoxy, aryl, aryl(1–6C)alkyl, heteroaryl, heteroaryl(1–6C)alkyl, heterocycle, cycloalkyl, alkenyl, alkynyl, adamantyl or polycycloalkyl.Type: GrantFiled: September 4, 2003Date of Patent: March 28, 2006Assignee: Aventis Pharma S.A.Inventors: Dominique Lesuisse, Gilles Dutruc-Rosset, Franck Halley, Didier Babin, Thomas Rooney, Gilles Tiraboschi
-
Patent number: 6962894Abstract: A selectively herbicidal composition for controlling grasses and weeds in crops of useful plants, comprising a) a herbicidally effective amount of a compound of formula I or a salt or diastereoisomer of a compound of formula I, and b) an amount, which is effective for antagonism of the herbicide, of a compound of formula IIaType: GrantFiled: September 5, 2000Date of Patent: November 8, 2005Assignee: Syngenta Crop Protection, Inc.Inventor: Jutta Glock
-
Patent number: 6960608Abstract: Novel fused indazoles and indoles are disclosed. Also disclosed are methods for the lowering and controlling of normal or elevated intraocular pressure as well as a method for the treatment of glaucoma using compositions containing one or more of the compounds of the present invention.Type: GrantFiled: November 25, 2003Date of Patent: November 1, 2005Assignee: Alcon, Inc.Inventors: Jesse A. May, Anura P. Dantanarayana
-
Patent number: 6927233Abstract: Compositions and methods for controlling intraocular pressure and treating glaucoma using 1-(2-aminopropyl)-indazol-6-ol are disclosed.Type: GrantFiled: November 14, 2000Date of Patent: August 9, 2005Assignees: Alcon, Inc., Yamanouchi Pharmaceutical Co., Ltd.Inventors: Jesse A. May, Anura P. Dantanarayana
-
Patent number: 6913759Abstract: A pharmaceutical composition having a gel consistency at room temperature and suitable for the treatment of a vaginal infection comprises, on a total composition weight basis, about 0.1 to about 3 weight percent of benzydamine hydrochloride, about 16 to about 35 weight percent of a polyoxyalkylene block copolymer, and about 2 to about 30 weight percent of propylene glycol, in water having a pH value in the range of about 3.5 to about 7. The weight ratio of water to polyoxyalkylene block copolymer in the composition is less than about 4:1. Optionally, the gel compositions can also contain glycerin, physiologically tolerable preservatives and buffers, as well as other pharmaceutically acceptable excipients.Type: GrantFiled: March 11, 2003Date of Patent: July 5, 2005Assignee: Curatek Pharmaceuticals Holding, Inc.Inventors: Robert J. Borgman, James E. Juul
-
Patent number: 6906070Abstract: The present application describes nitrogen containing heteroaromatics and derivatives thereof of formula I: or pharmaceutically acceptable salt forms thereof, wherein rings D-E represent guanidine mimics, which are useful as inhibitors of factor Xa.Type: GrantFiled: August 8, 2001Date of Patent: June 14, 2005Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Patrick Y. Lam, Charles G. Clark, Celia Dominguez, John M. Fevig, Qi Han, Renhua Li, Donald J. P. Pinto, James R. Pruitt, Mimi L. Quan