Abstract: Carboxylic acid amides of general formula having an antithrombotic activity and a factor Xa-inhibiting activity. Exemplary are: (a) N-[1-(3-amidino-phenyl)-2-(1H-tetrazol-5-yl)-ethyl]-4-(2,5-dihydro-pyrrol-1-yl-carbonyl)-3-methyl-benzamide, (b) N-[1-(3-amidino-phenyl)-2-(1H-tetrazol-5-yl)-ethyl]-3-methyl-4-(pyrrolidin-1-yl-carbonyl)-benzamide, (c) N-[1-(5-amidino-2-hydroxy-phenyl)-2-phenyl-ethyl]-3-methyl-4-(pyrrolidin-1-yl-carbonyl)-benzamide, and (d) N-[1-(5-amidino-2-hydroxy-phenyl)-2-(pyridin-3-yl)-ethyl]-3-methyl-4-(pyrrolidin-1-yl-carbonyl)-benzamide.
Type:
Grant
Filed:
July 21, 2003
Date of Patent:
January 4, 2005
Assignee:
Boehringer Ingelheim Pharma GmbH & Co. KG
Inventors:
Uwe Ries, Henning Priepke, Wolfgang Wienen, Herbert Nar, Sandra Handschuh
Abstract: Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating coagulation disorders.
Type:
Grant
Filed:
October 15, 2003
Date of Patent:
December 28, 2004
Assignee:
Millennium Pharmaceuticals, Inc.
Inventors:
Bing-Yan Zhu, Penglie Zhang, Lingyan Wang, Wenrong Huang, Erick A. Goldman, Wenhao Li, Jingmei Zuckett, Yonghong Song, Robert M. Scarborough
Abstract: This invention pertains to compounds of Formula I, their N-oxides and suitable salts (Formula I) wherein A is O or S; G is a 5- or 6-membered heteroaromatic ring or a 5- or 6-membered nonaromatic heterocyclic ring optionally including one or two ring members selected from the group consisting of C(═O), SO or S(O)2, each ring optionally substituted with from one to four R2; each J is independently a phenyl ring, a 5- or 6-membered heteroaromatic ring or an aromatic 8-, 9- or 10-membered fused carbobicyclic or heterobicyclic ring system, wherein each ring or ring system is optionally substituted with from one to four R3; and R1, R2, R3, R4 and n are as defined in the disclosure. Also disclosed are methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound of Formula I, an N-oxide thereof or a suitable salt of the compound (e.g., as a composition described herein).
Type:
Application
Filed:
June 9, 2004
Publication date:
December 2, 2004
Inventors:
David Alan Clark, Bruce Lawrence Finkelstein, George Philip Lahm, Thomas Paul Selby, Thomas Martin Stevenson
Abstract: The present invention relates to a &bgr;3 adrenergic receptor agonist of formula I: 1
Type:
Application
Filed:
May 4, 2004
Publication date:
December 2, 2004
Inventors:
Britta Evers, Cynthia Darshini Jesudason, Rushad Eruch Karanjawala, David Michael Remick, Gerd Ruehter, Daniel Jon Sall, Theo Schotten, Miles Goodman Siegel, Wolfgang Stenzel, Russell Dean Stucky, John Arnold Werner
Abstract: The present invention includes compounds of pyridinium salts and methods of their use for industrial uses. The present invention also relates to methods of controlling fungi and/or bacteria. The present invention may also be used to control insects.
Type:
Application
Filed:
March 3, 2004
Publication date:
November 25, 2004
Inventors:
Richard B. Klein, Jeffrey L. Selph, John J. Partridge, John Reinhard
Abstract: A peroxisome proliferator activated receptor regulator containing a compound of formula (I)
(wherein all symbols are as defined in the specification), or a salt thereof as active ingredient.
Because of having an effect of regulating PPAR, a compound of formula (I) is useful as a hypoglycemic agent, a hypolipidemic agent, a preventive and/or a remedy for diseases associating metabolic disorders (diabetes, obesity, syndrome X, hypercholesterolemia, hyperlipoproteinemia, etc.), hyperlipemia, atherosclerosis, hypertension, circulatory diseases, overeating, coronary heart diseases, etc., an HDL cholesterol-elevating agent, an LDL cholesterol and/or VLDL cholesterol-lowering agent and a drug for relief from risk factors of diabetes or syndrome X.
Abstract: The invention relates to substituted N-aryl heterocycles and to the physiologically tolerated salts and physiologically functional derivatives thereof.
Type:
Application
Filed:
February 17, 2004
Publication date:
November 4, 2004
Applicant:
Aventis Pharma Deutschland GmbH
Inventors:
Lothar Schwink, Siegfried Stengelin, Matthias Gossel, Thomas Boehme, Gerhard Hessler, Petra Stahl, Dirk Gretzke
Abstract: The present invention relates to compounds useful of inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
Type:
Application
Filed:
March 11, 2004
Publication date:
November 4, 2004
Inventors:
Francois Maltais, Alex Aronov, Michael R. Hale, Young-Choon Moon
Abstract: In one aspect, the present invention concerns the use of certain quaternary ammonium compounds as active ingredient in the manufacture of a medicament for use in the treatment and/or prevention of cough in warm-blooded animals, including humans, such as compounds of the following formula (I): Y-J-E An− wherein J is independently selected from a group represented by one of formulae (II), (III) and (IV).
Type:
Application
Filed:
February 14, 2003
Publication date:
October 28, 2004
Inventors:
Lewis Siu Leung Choi, Gregory N Beatch, Clive Page
Abstract: Compounds and their use as pharmaceuticals particularly as Raf kinase inhibitors for the treatment of neurotraumatic diseases, cancer, chronic neurodegeneration, pain, migraine or cardiac hypertrophy.
Type:
Application
Filed:
March 4, 2004
Publication date:
September 30, 2004
Inventors:
David Kenneth Dean, Andrew Kenneth Takle, David Matthew Wilson
Abstract: This invention relates to pyrazole derivatives of 1
Type:
Application
Filed:
March 15, 2004
Publication date:
September 16, 2004
Inventors:
Uday Khire, Chengzhi Zhang, Harold C E Kluender, Ingo Mugge, Zhengqui Hong, Jianxing Shao, Neil Bifulco, Pamela A Trail, Jacques Dumas, Rico C Lavoie, Xaio-Gao Liu, Veena Agarwal, Sharad K Verma, Lei Wang
Abstract: The subject invention provides pharmaceutical compounds useful in the treatment of Type II diabetes. These compounds are advantageous because they are readily metabolized by the metabolic drug detoxification systems. Particularly, isoxazolidine compounds which have been designed to include esters within the structure of the compounds are provided. This invention is also drawn to methods of treating disorders, such as diabetes, comprising the administration of therapeutically effective compositions comprising compounds which have been designed to be metabolized by serum or intracellular hydrolases and esterases. Pharmaceutical compositions of the isoxazolidine compounds are also taught.
Abstract: A chemical genus of 2-(aminomethyl)arylamides, which are useful as analgesics, is disclosed.
Type:
Application
Filed:
February 11, 2003
Publication date:
August 26, 2004
Applicant:
PHARMACOPEIA, INC
Inventors:
Koc-Kan Ho, John J. Baldwin, Adolph C. Bohnstedt, Steven G. Kultgen, Edward McDonald, Tao Guo, John Richard Morphy, Zoran Rankovic, Robert Horlick, Kenneth C. Appell
Abstract: Novel pyrrolidine compounds that are potent and selective inhibitors of PDE4, as well as methods of making the same, are disclosed. Use of the compounds in the treatment of inflammatory diseases and other diseases involving elevated levels of cytokines, as well as central nervous system (CNS) disorders, also is disclosed.
Type:
Application
Filed:
January 15, 2004
Publication date:
August 5, 2004
Inventors:
Timothy J. Martins, Kerry W. Fowler, Joshua Odingo, Edward A. Kesicki, Amy Oliver, Laurence E. Burgess, John J. Gaudino, Zachary S. Jones, Bradley J. Newhouse, Stephen T. Schlachter
Abstract: Aminopyridine derivatives of the following formula I which exhibit pharmacological activity at estrogen receptors alpha (ER&agr;) and beta (ER&bgr;) are described herein. The described invention also includes compositions and medicaments containing the aminopyridine derivatives as well as processes for the preparation and use of such compounds, compositions and medicaments.
Type:
Application
Filed:
March 23, 2004
Publication date:
August 5, 2004
Inventors:
David Harold Drewry, Brad Richard Henke
Abstract: This invention provides a class of androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds, which are selective androgen receptor modulators (SARM). Several of the SARM compounds have been found to have an unexpected androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. Other SARM compounds have been found to have an unexpected antiandrogenic activity of a nonsteroidal ligand for the androgen receptor.
Abstract: Methods of treating cyclooxygenase-2 mediated disorders comprising administering to a subject a therapeutically effective amount of one or more fluoro-substituted benzenesulfonyl compounds corresponding to Formula I: 1
Type:
Application
Filed:
December 12, 2003
Publication date:
July 15, 2004
Applicant:
Pharmacia Corporation
Inventors:
David L. Brown, Matthew J. Graneto, Cindy L. Ludwig, John M. Molyneaux, John J. Talley
Abstract: The present invention relates to certain substituted pyrroles which modulate the activity of protein kinases (“PKs”). The compounds of this invention are therefore useful in treating disorders related to abnormal PK activity. Pharmaceutical compositions comprising these compounds, methods of treating diseases utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.
Type:
Application
Filed:
October 7, 2003
Publication date:
July 15, 2004
Applicant:
Sugen, Inc.
Inventors:
Connie Li Sun, Peng Cho Tang, Denise Ockey
Abstract: Novel pyrazole compounds, including derivatives thereof, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use are described. The compounds of the present invention are potent inhibitors of transforming growth factor (“TGF”)-&bgr; signaling pathway. They are useful in the treatment of various TGF-related disease states including, for example, cancer, and fibrotic diseases.
Abstract: Bombesin receptor antagonists are provided which are useful for the diagnosis, prevention, or treatment of male sexual dysfunction in humans and animals, female sexual dysfunction in humans and animals, anxiety and panic disorders, social phobia, depression, psychoses, sleeping disorders, memory impairment, pulmonary hypertension, lung repair and lung development disorders, cancer including prostate cancer and pancreatic cancer, hepatic porphyria, gastrointestinal secretory disturbances, gastrointestinal disorders including colitis, Crohn's disease and inflammatory bowel disease, emesis, anorexia, pain, seasonal affective disorders, feeding disorders, or pruritus.
Type:
Application
Filed:
December 4, 2003
Publication date:
June 17, 2004
Inventors:
Michael Higginbottom, Martyn Clive Pritchard, Herman Thijs Stock
Abstract: A method of producing a 6-substituted (S)-nicotine derivative with the general formula (III), wherein R is an optionally substituted alkyl, alkenyl, alkynyl, amido or amino group, optionally coupled to a carrier protein, is disclosed. An intermediate compound useful in the method is also comprised by the invention. The formula of the compound is (A) in which A represents the cationic radical of an organic nitrogen base, Y represents an anion formed by an electrophilic compound.
Abstract: The present invention relates to a compound of the formula (I)wherein R1 is benzofuranyl substituted by halogen, or styryl substituted by halogen; R2 is substituted hydroxy, substituted mercapto or substituted sulfonyl; and X is or pharmaceutically acceptable salts thereof. The compound (1) of the present invention and pharmaceutically acceptable salts thereof possess a strong inhibitory activity on the production of nitric oxide (NO), and are useful for prevention and/or treatment of NO-mediated diseases in human being and animals.
Abstract: The present invention relates to new hetaryl-substituted homotetramic and homotetronic acids of the formula (I) 1
Type:
Application
Filed:
November 24, 2003
Publication date:
May 20, 2004
Inventors:
Reiner Fischer, Astrid Ullmann, Axel Trautwein, Mark Wilhelm Drewes, Christoph Erdelen, Peter Dahmen, Dieter Feucht, Rolf Pontzen, Peter Losel
Abstract: Disclosed are novel pyrrole derivatives, a process for their manufacture, pharmaceutical compositions containing such compounds and the use of such compounds in the treatment of HIV mediated diseases.
Type:
Grant
Filed:
June 13, 2001
Date of Patent:
May 18, 2004
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Brian William Dymock, Philip Stephen Jones, John Herbert Merrett, Martin John Parratt
Abstract: Benzanilides are provided which are voltage-dependent potassium channel openers. Methods of using the benzanilides of the invention are also provided.
Type:
Grant
Filed:
November 1, 2001
Date of Patent:
May 18, 2004
Assignee:
ICAgen, Inc.
Inventors:
Grant A. McNaughton-Smith, Michael F. Gross, Alan D. Wickenden
Abstract: A compound of formula (1) wherein R1 is hydrogen, halo or methoxy, R2 is hydrogen, halo, methyl, ethyl or methoxy; R3 is carboxy, tetrazolyl, or —CONHSO2R4 where R4 is methyl, ethyl, phenyl, 2,5-dimethylisoxazolyl or trifluoromethyl; T is —CH2— or —SO2—; and ring A is 3-chlorophenyl, 4-chlorophenyl, 3-trifluoromethylphenyl, 3,4-dichlorophenyl, 3,4-difluorophenyl, 3-fluoro-4-chlorophenyl, 3-chloro-4-fluorophenyl or 2,3-dichloropyrid-5-yl; or a pharmaceutically acceptable salt or prodrug thereof, as well as pharmaceutical compositions containing them are described and claimed. These compounds and compositions are useful in the treatment of disease mediated by monocyte chemoattractant protein-1 or RANTES (Regulated Upon Activation, Normal T-cell Expressed and Secreted), such as inflammatory disease.
Abstract: The present invention relates to a mutual prodrug of amlodipine and atorvastatin, pharmaceutically acceptable acid addition salts thereof, pharmaceutical compositions thereof and the use of said prodrug and its salts in the manufacture of medicaments for the treatment of atherosclerosis, angina pectoris, combined hypertension and hyperlipidaemia and the management of cardiac risk.
Abstract: The invention relates to a convergent process for preparing a compound of the formula (V), wherein R1 is attached at the 2 or 3 position of the benzene ring, R2 is attached at the 5 or 6 position and R1, R2 and G are as defined herein, in which an aryl boronic acid is coupled with an amine protected halo-substituted-2-aminopyridine using a palladium coupling agent. Compounds of formula V are useful as nitric oxide synthase (NOS) inhibitors in a mammal.
Abstract: Methods of treating cyclooxygenase-2 mediated disorders comprising administering to a subject a therapeutically effective amount of one or more 2-fluorobenzenesulfonyl compounds corresponding to Formula (I) wherein A, R1, R2, and R3 are as described in the specification, and novel 2-fluorobenzenesulfonyl compounds within Formula (I).
Type:
Application
Filed:
July 11, 2003
Publication date:
May 13, 2004
Inventors:
David L. Brown, Matthew J. Graneto, Cindy L. Ludwig, John J. Talley
Abstract: The present invention provides 2-methoxyimino-2-(pyridinyloxymethyl) phenyl acetamides according to formula (I) as well as their use as fungicidal compounds.
Type:
Grant
Filed:
February 27, 2003
Date of Patent:
May 11, 2004
Assignee:
Dow AgroSciences LLC
Inventors:
Neil Vincent Kirby, Jenifer Lynn Adamski Butz, Brent Jeffrey Rieder, James M. Renga, Jeannie Rachel Phillips Cetusic, Irene Mae Morrison, John Todd Mathieson, Gary David Gustafson
Abstract: The present invention is related to sulfonamide derivatives having a lipophilic moiety and which are substantially soluble. Said compounds are notably for use as pharmaceutically active compounds. The present invention also related to pharmaceutical formulations containing such sulfonamide derivatives. Said sulfonamide derivatives are efficient modulators of the JNK pathway, they are in particular efficient and selective inhibitors of JNK 2 and 3. The present invention is furthermore related to novel sulfonamide derivatives as well as to methods of their preparation.
Type:
Application
Filed:
October 10, 2003
Publication date:
April 22, 2004
Inventors:
Serge Halazy, Dennis Church, Stephen J. Arkinstall, Marco Biamonte, Montserrat Camps, Jean-Pierre Gotteland, Thomas Rueckle
Abstract: The present invention provides an excellent squalene synthase inhibitor. Specifically, it provides a compound (I) represented by the following formula, a salt thereof or a hydrate of them.
Abstract: The present application describes novel spiro-cyclic &bgr;-amino acid derivatives of formula I:
or pharmaceutically acceptable salt forms thereof, wherein ring B is a 3-13 membered carbocycle or heterocycle, ring C forms a 3-11 membered spiro-carbocycle or spiro-heterocycleon ring B, and the other variables are defined in the present specification, which are useful as as matrix metalloproteinases (MMP), TNF-&agr; converting enzyme (TACE), and/or aggrecanase inhibitors.
Type:
Grant
Filed:
March 12, 2002
Date of Patent:
April 13, 2004
Assignee:
Bristol-Myers Squibb Pharma
Inventors:
Gregory R. Ott, Xiao Tao Chen, Jingwu Duan, Matthew E. Voss
Abstract: An alkanoic acid derivative useful as a prophylactic or therapeutic agent of diabetes mellitus, hyperlipidemia, impaired glucose tolerance and the like can be provided by a compound represented by the formula 1
Abstract: The present invention relates to compounds of the formula (I) wherein R1 and R2 are each independently lower alkyl lower alkenyl, acyl, amino, lower alkoxy, lower cycloalkyloxy, aryl, aryloxy, sulfooxy, mercapto, sulfo, hydrogen, halogen, nitro, cyano or hydroxy, or may form a ring structure; Q1 is N or CH; L is optionally substituted unsaturated 3 to 10-membered heterocyclic group; X is optionally substituted monocyclic arylene or monocyclic heteroarylene; Y is -(A1)m-(A2)n-(A4)k-; Z is directbond, —CH2-, —NH— or —O—; and R is hydrogen or lower alkyl, or a salt thereof The compounds of the present invention inhibit apolipoprotein B (Apo B) secretion and are useful as a medicament for prophylactic and treatment of diseases or conditions resulting from elevated circulating levels of Apo B.
Abstract: The present application describes modulators of CCR3 of formula (I):
or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.
Type:
Grant
Filed:
June 26, 2002
Date of Patent:
March 16, 2004
Assignee:
Bristol-Myers Squibb Pharma Company
Inventors:
Paul S. Watson, Soo S. Ko, George V. DeLucca, John V. Duncia, Joseph B. Santella, III, Dean A. Wacker