Abstract: The invention is directed to physiologically active compounds of the general formula (Ix) and compositions containing such compounds, and their prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their prodrugs, as well as to novel compounds within the scope of formula (Ix), and to processes for their preparation. Such compounds and compositions have valuable pharmaceutical properties, in particular the ability to inhibit kinases.
Type:
Grant
Filed:
October 24, 2002
Date of Patent:
May 24, 2005
Assignee:
Aventis Pharmaceuticals Inc.
Inventors:
Michael L. Edwards, Paul J. Cox, Shelley Amendola, Stephanie D. Deprets, Timothy A. Gillespy, Christopher D. Edlin, Andrew D. Morley, Charles J. Gardner, Brian Pedgrift, Herve Bouchard, Didier Babin, Laurence Gauzy, Alain Le-Brun, Tahir N. Majid, John C. Reader, Lloyd J. Payne, Nawaz M. Khan, Michael Cherry
Abstract: The present application describes novel hydantoin derivatives of formula (I): or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, B, R1, R2, R3, R4, R5, R6, R7, R11, and n are defined in the present specification, which are useful as inhibitors of matrix metalloproteinases (MMP), TNF-? converting enzyme (TACE), aggrecanase, or a combination thereof.
Type:
Grant
Filed:
May 23, 2002
Date of Patent:
May 10, 2005
Assignee:
Bristol-Myers Squibb Pharma Company
Inventors:
James E. Sheppeck, Jingwu Duan, Chu-Biao Xue, Zelda Wasserman
Abstract: The present invention relates to dopamine D4 ligands having the general formula I wherein R1—R10, W, X, Y1—Y4, and n are as described herein. The compounds of the invention are potent dopamine D4 receptor ligands.
Type:
Grant
Filed:
December 9, 2002
Date of Patent:
May 10, 2005
Assignee:
H. Lundbeck A/S
Inventors:
Benny Bang-Andersen, Jakob Felding, Jan Kehler, Kim Andersen
Abstract: Compounds having the formula are methionine aminopeptidase type 2 (MetAP2) inhibitors and are useful for inhibiting angiogenesis. Also disclosed are MetAP2-inhibiting compositions and methods of inhibiting angiogenesis in a mammal.
Type:
Grant
Filed:
February 19, 2004
Date of Patent:
May 3, 2005
Assignee:
Abbott Laboratories
Inventors:
Richard A. Craig, Megumi Kawai, Linda M. Lynch, Jyoti R. Patel, George S. Sheppard, Jieyi Wang, Fan Yang, Nwe Ba-Maung, Xenia Beebe Searle
Abstract: The present invention relates to novel cinnamide compounds that are useful for treating inflammatory and immunune diseases, to pharmaceutical compositions containing these compounds, and to methods of inhibiting inflammation or suppressing immune response in a mammal.
Type:
Grant
Filed:
March 31, 2000
Date of Patent:
April 12, 2005
Assignee:
Abbott Laboratories
Inventors:
James Link, Gang Liu, ZhongHua Pei, Tom von Geldern, Martin Winn, Zhili Xin, Steven A. Boyd, Gui-Dong Zhu, Jennifer C. Freeman, Indrani W. Gunawardana, Michael A. Staeger, Hwan-Soo Jae, John K. Lynch, Sheldon Wang
Abstract: A novel class of compounds, which act to antagonize the action of the glucagon hormone on the glucagon receptor. Owing to their antagonizing effect of the glucagon receptor the compounds may be suitable for the treatment and/or prevention of any glucagon-mediated conditions and diseases such as hyperglycemia, Type 1 diabetes, Type 2 diabetes and obesity.
Type:
Grant
Filed:
August 30, 2002
Date of Patent:
April 5, 2005
Assignee:
Novo Nordisk A/S
Inventors:
Jesper Lau, Peter Madsen, Christian Sams, Carsten Behrens, Inge Thøger Christensen, Behrend Frederik Lundt, Ulla Grove Sidelmann, Henning Thøgersen, Anthony L. Ling, Michael Bruno Plewe, Larry Kenneth Truesdale, Anker Steen Jøgensen, Janos Tibor Kodra, Shenghua Shi
Abstract: A method for the treatment of cancer and pain in an animal subject is disclosed, comprising administering to said animal in need of such treatment an effective amount of a compound of formula I: wherein R1-R6 are defined herein. Pharmaceutical compositions comprising one or more compounds of formula I and a pharmaceutically acceptable carrier are also disclosed.
Abstract: Condensed pyridine compounds represented by formula (I): wherein: R1 and R3 are, independently, hydrogen, lower alkyl, or lower alkoxy; R2 represent an amino substituent; ring A is a benzene ring, pyridine ring, thiophene ring, or furan ring; and B represents a substituent containing a ring structure. Also, pharmaceutically acceptable salt and hydrates thereof. These compounds are clinically useful medicaments having serotonin antagonism, and in particular, for treating, ameliorating, or preventing spastic paralysis. They are also useful as central muscle relaxants for ameliorating myotonia.
Abstract: One aspect of the present invention relates to heterocyclic compounds comprising a sulfonamide moiety. A second aspect of the present invention relates to the use of the heterocyclic compounds comprising a sulfonamide moiety to treat diseases, afflictions or maladies caused at least in part by abnormal activity of one or more GPCRs or ligand-gated ion channels. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds comprising a sulfonamide moiety, and the screening of those libraries for biological activity, e.g., in animal models of psychosis.
Type:
Grant
Filed:
January 28, 2004
Date of Patent:
March 29, 2005
Assignee:
Sepracor, Inc.
Inventors:
Xinhe Wu, Brian M. Aquila, Liming Shao, Heike Radeke, Gregory D. Cuny, James R. Hauske, Roger L. Xie
Abstract: This invention is directed to sorbitol dehydrogenase inhibitory compounds of the formula I, wherein R1, R2 and R3 are as defined in the specification. This invention is also directed to pharmaceutical compositions containing those compounds and methods of treating or preventing diabetic complications, particularly diabetic neuropathy, diabetic nephropathy, diabetic microangiopathy, diabetic macroangiopathy and diabetic cardiomyopathy by administering such compounds to a mammal suffering from diabetes and therefore at risk for developing such complications. This invention is also directed to pharmaceutical compositions comprising a combination of compound of formula I of this invention with an aldose reductase inhibitor and to methods of treating or preventing diabetic complications therewith.
Type:
Grant
Filed:
August 21, 2003
Date of Patent:
March 22, 2005
Assignee:
Pfizer Inc
Inventors:
Margaret Y. Chu-Moyer, Jerry A. Murry, Banavara L. Mylari, William J. Zembrowski
Abstract: This invention is directed to methods of treating insulin resistance in a mammal which comprise administering an effective amount of a compound of formula I, where the variables are defined in the specification, or the stereoisomeric mixtures, diastereomerically enriched, diastereomerically pure, enantiomerically enriched or enantiomerically pure isomers, or the pharmaceutically acceptable salts and prodrugs thereof to said mammal. The compounds of formula I are growth hormone secretagogues and as such are useful for increasing the level of endogenous growth hormone. In another aspect this invention provides certain intermediates which are useful in the synthesis of the foregoing compounds and certain processes useful for the synthesis of said intermediates and th compounds of formula I. This invention is further directed to methods comprising administering to a human or other animal a combination of a functional somatostatin antagonist such as an alpha-2 adrenergic agonist and a compound of formula I.
Type:
Grant
Filed:
July 22, 2003
Date of Patent:
March 15, 2005
Assignee:
Pfizer Inc.
Inventors:
Philip Albert Carpino, Charles Kwok-Fung Chiu, Lydia Codetta Pan, Bruce Allen Lefker, Judith Lee Treadway, Michael Paul Zawistoski
Abstract: The present invention relates to novel cinnamide compounds that are useful for treating inflammatory and immune diseases and cerebral vasospasm, to pharmaceutical compositions containing these compounds, and to methods of inhibiting inflammation or suppressing immune response in a mammal.
Abstract: The invention relates to compounds of the formula 1 and to pharmaceutically acceptable salts and solvates thereof, wherein A, X, R1, R3 and R4 are as defined herein. The invention also relates to methods of treating abnormal cell growth in mammals by administering the compounds of formula 1 and to pharmaceutical compositions for treating such disorders which contain the compounds of formula 1. The invention also relates to methods of preparing the compounds of formula 1.
Type:
Grant
Filed:
August 22, 2002
Date of Patent:
March 15, 2005
Assignee:
Pfizer Inc
Inventors:
John Charles Kath, Norma Jacqueline Tom, Eric David Cox, Samit Kumar Bhattacharya
Abstract: The present invention provides novel compounds of the Formula (I): A-B, its prodrug forms, or pharmaceutically acceptable salts thereof, wherein A represents a saturated, unsaturated, or a partially unsaturated bicyclic heterocyclic ring structure, and B represents an aryl or a heteroaryl group. Preferred compounds of the present invention comprise a benzimidazole or indole nucleus. The compounds of this invention are inhibitors of serine proteases, Urokinase (uPA), Factor Xa (FXa), and/or Factor VIIa (FVIIa), and have utility as anti cancer agents and/or as anticoagulants for the treatment or prevention of thromboembolic disorders in mammals.
Type:
Grant
Filed:
December 17, 1999
Date of Patent:
March 15, 2005
Assignee:
Axys Pharmaceuticals, Inc.
Inventors:
Darin A. Allen, Jason M. Hataye, Witold N. Hruzewicz, Aleksandr Kolesnikov, Richard L. Mackman, Roopa Rai, Spencer R. Jeffrey, Erik J. Verner, Wendy B. Young, William Dvorak Shrader
Abstract: The invention pertains, at least in part, to new intermediates and synthetic methods for the stereospecific synthesis of oxazinone compounds, which are useful, for example, as antibiotics. The invention also pertains to novel olefinic oxazinone compounds, methods for their synthesis, and methods of using these compounds for the synthesis of oxazinones. The invention also pertains to methods for using the compounds to treat bacterial associated states in subjects.
Abstract: The present invention relates to 4-arylindolinones, as well as pharmaceutical compositions thereof, capable of modulating protein kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation. The present invention also relates to methods for treating protein kinase related disorders.
Type:
Grant
Filed:
December 16, 2003
Date of Patent:
March 1, 2005
Assignee:
Sugen, Inc.
Inventors:
Jingrong Cui, Ruofei Zhang, Hong Shen, Ji Yu Chu, Fang-Jie Zhang, Marcel Koenig, Steven Huy Do, Xiaoyuan Li, Chung Chen Wei, Peng Cho Tang
Abstract: Disclosed are compounds that inhibit the microbial NAD synthetase enzyme. For example, disclosed are compounds of the formula Ar1—X—Ar2—Y—L—Z—Q, wherein Q is Q1Ar3 or Ar3Q1; Ar1, Ar2, and Ar3 are independently aryl or heteroaryl, optionally substituted with one or more substituents; X, Y, and Z are independently selected from the group consisting of a covalent bond or groups containing one or more of C, H, N, O, S atoms; L is a linker and Q1 is an alkylenyl, alkylenyl carbonyloxy alkyl, or alkylenyl carbonylamino alkyl group, optionally having a substituent; a covalent bond; a group containing amidine or guanidine function wherein the amidine or guanidine may be optionally N-substituted with an alkyl; or a zwitterion; or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
February 22, 2002
Date of Patent:
March 1, 2005
Assignees:
Virtual Drug Development, Inc., The UAB Research Foundation
Inventors:
Wayne J. Brouillette, Lawrence DeLucas, Christie Brouillette, Sadanandan E. Velu, Yong-Chul Kim, Liyuan Mou, R. Stephen Porter
Abstract: Compounds useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis, are disclosed.
Abstract: A method of using an MMP inhibitor and optionally radiation therapy, and one or more antineoplastic agents of the topoisomerase class selected from the group consisting of irinotecan and topotecan, as a combination therapy for the treatment of neoplasia is disclosed.
Type:
Grant
Filed:
December 22, 1999
Date of Patent:
February 22, 2005
Assignee:
G. D. Searle & Co.
Inventors:
John P. McKearn, Gary Gordon, James J. Cunningham, Stephen T. Gately, Alane T. Koki, Jaime L. Masferrer