Abstract: This invention relates to mutual prodrugs of amlodipine and atorvastatin and to pharmaceutical compositions thereof. This invention also relates to methods of treating angina pectoris, atherosclerosis, and hypertension and hyperlipidemia in a mammal using those prodrugs and compositions. This invention also relates to methods of managing cardiac risk in a mammal, including humans, presenting with symptoms of cardiac risk by administering those prodrugs and compositions.
Type:
Grant
Filed:
May 24, 2000
Date of Patent:
November 26, 2002
Assignee:
Pfizer Inc
Inventors:
George Chang, Ernest S. Hamanaka, John L. LaMattina
Abstract: Novel prodrugs of amino ceramide-like compounds are provided which inhibit glucosyl ceramide (GlcCer) formation by inhibiting the enzyme GlcCer synthase, thereby lowering the level of glycosphingolipids. The compounds of the present invention have improved GlcCer synthase inhibition activity and are therefore highly useful in therapeutic methods for treating various conditions and diseases associated with altered glycosphingolipid levels.
Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt thereof:
wherein R1, R2 and R3 are various substituent groups; and
one of X1 and X2 is N or CR′, and the other is NR′ or CHR′ wherein R′ is hydrogen, OH, C1-6alkyl, or C3-7cycloalkyl; or when one of X1 and X2 is N or CR′ then the other may be S or O;
and their use as pharmaceuticals.
Abstract: The present invention relates to certain 6-phenyl-pyridin-2-ylamine derivatives that exhibit activity as nitric oxide synthase (NOS) inhibitors, to pharmaceutical compositions containing them and to their use in the treatment and prevention of central nervous system disorders.
Abstract: The present invention relates to novel 2-aminopyridine derivative compounds of the following formula:
wherein R1 to R5 have the meanings provided herein. The invention further relates to combinatorial libraries containing two or more such compounds, as well as methods of preparing 2-aminopyridine derivative compounds.
Type:
Grant
Filed:
September 29, 1999
Date of Patent:
October 1, 2002
Assignee:
Lion Bioscience AG
Inventors:
Behrouz Forood, Brenton T. Flatt, Christophe Chassaing, Alan K. Katritzky
Abstract: The invention concerns amide derivatives of formula (I)
wherein R3 is (1-6C)alkyl or halogeno; m is 0-3, p is 0-2 and q is 0-4; each of R1 and R2 is a group such as hydroxy, halogeno, trifluoromethyl and cyano; R4 is a basic group such as amino, (1-6C)alkylamino, di-[(1-6C)alkyl]amino, di-[(1-6C)alkyl]amino-(1-6C)alkyl, di-[(1-6C)alkyl]amino-(2-6C)alkoxy, heteroaryl, heteroaryloxy, heteroaryl-(1-6C)alkoxy, heterocyclyl, heterocyclyloxy and heterocyclyl-(1-6C)alkoxy; and Q2 is a group such as heteroaryl, heteroaryloxy or heteroaryl-(1-6C)alkoxy which is optionally substituted; or pharmaceutically-acceptable salts or in-vivo-cleavable esters thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.
Abstract: Compounds of Formula I have activity as inhibitors of binding between VCAM-1 and cells expressing VLA-4 and are useful for treating disease whose symptoms and or damage are related to the binding of VCAM-1 to cells expressing VLA-4.
Type:
Application
Filed:
January 29, 2002
Publication date:
September 19, 2002
Inventors:
Gerald Lewis Kaplan, Achyutharao Sidduri, Jefferson Wright Tilley
Abstract: A process is provided for preparing a compound of the formula:
using a compound having the formula
wherein R2 and R3 are independently C1-C3 alkyl or phenyl.
Abstract: The present invention relates to the potentiation of glutamate receptor function using certain sulphonamide derivatives. It also relates to novel sulphonamide derivatives, to processes for their preparation and to pharmaceutical compositions containing them.
Type:
Application
Filed:
January 18, 2002
Publication date:
August 22, 2002
Inventors:
MacKlin Brian Arnold, Paul Leslie Ornstein, Richard Lee Simon, Hamideh Zarrinmayeh, Dennis Michael Zimmerman
Abstract: Novel 3-pyridyloxymethyl heterocyclic ether compounds of the formula:
or the pharmaceutically-acceptable salts or prodrugs thereof are selective and potent ligands at neuronal nicotinic cholinergic channel receptors, and are effective in controlling synaptic transmission. Key intermediates and processes using this key intermediates to produce compounds of formula I with the variables defined in the specification are also described.
Type:
Grant
Filed:
March 1, 2000
Date of Patent:
August 20, 2002
Assignee:
Abbott Laboratories
Inventors:
Nan-Horng Lin, Yun He, Mark W. Holladay, Keith Ryther, Yihong Li, Hao Bai
Abstract: The present invention is a series of compounds formed from phenyl substituted pyridine or benzene derivatives and their pharmaceutically acceptable salts. These compounds have shown high affinity as antagonists to the NK-1 receptor.
Type:
Application
Filed:
January 17, 2002
Publication date:
August 15, 2002
Inventors:
Michael Bos, Guido Galley, Thierry Godel, Torsten Hoffmann, Walter Hunkeler, Patrick Schnider, Heinz Stadler
Abstract: The present application de gibes novel cyclic hydroxamic acids of formula I:
or pharmaceutically acceptable salt forms thereof, wherein ring B is a 5-7 membered cyclic system containing from 0-2 heteroatoms selected from O, N, NRa, and S(O)p, and 0-1 carbonyl groups and the other variables are defined in the present specification, which are useful as metalloprotease inhibitors.
Type:
Grant
Filed:
June 17, 1999
Date of Patent:
August 6, 2002
Inventors:
Chu-Biao Xue, Carl P. Decicco, Xiaohua He
Abstract: The present invention provides of method of preparing phenyl-substituted azoles. This method uses an efficient ligand-accelerated Ullmann coupling reaction of anilines with azoles. The coupling products are useful for preparing factor Xa inhibitors.
Type:
Application
Filed:
July 25, 2001
Publication date:
July 25, 2002
Inventors:
Jiacheng Zhou, Pasquale N. Confalone, Hui-Yin Li, Philip Ma, Lynette M. Oh, Lucius T. Rossano, Charles G. Clark, Chris Teleha
Abstract: Racemates, diastereoisomers and optical isomers of a compound of formula (I):
wherein
B is H, a C6 or C10 aryl, C7-16 aralkyl; Het or (lower alkyl)-Het, all of which optionally substituted with C1-6 alkyl; C1-6 alkoxy; C1-6 alkanoyl; hydroxy; hydroxyalkyl; halo; haloalkyl; nitro; cyano; cyanoalkyl; amino optionally substituted with C1-6 alkyl; amido; or (lower alkyl)amide; or
B is an acyl derivative of formula R4—C(O)—; a carboxyl of formula R4—O—C(O)—; an amide of formula R4—N(R5)—C(O)—; a thioamide of formula R4—N(R5)—C(S)—; or a sulfonyl of formula R4—SO2; R5 is H or C1-6 alkyl; and
Y is H or C1-6 alkyl;
R3 is C1-8 alkyl, C3-7 cycloalkyl, or C4-10 alkylcycloalkyl, all optionally substituted with hydroxy, C1-6 alkoxy, C1-6 thioalkyl, amido, (lower alkyl)amido, C6 or C10 aryl, or C7-16 aralkyl;
R2 is CH2—R20, NH—R20, O—R20 or S—R20, wherein R20 is a saturated or unsaturated C3-7 cycloalkyl o
Type:
Grant
Filed:
April 6, 2001
Date of Patent:
July 16, 2002
Assignee:
Boehringer Ingelheim (Canada) Ltd.
Inventors:
Montse Llinas-Brunet, Murray D. Bailey, Dale R. Cameron, Ellse Ghiro, Nathalie Goudreau, Marc-Andre Poupart, Jean Rancourt, Youla S. Tsantrizos, Anne-Marie Faucher, Teddy Halmos, Dominik M. Wernic
Abstract: The invention provides compounds which are useful as inhibitors of metalloproteases, and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the present invention relates to a compound having a structure according to Formula (I).
Also disclosed are compounds, pharmaceutical compositions and methods of treating diseases characterized by metalloprotease activity using these compounds or the pharmaceutical compositions containing them.
Type:
Grant
Filed:
August 26, 1997
Date of Patent:
July 9, 2002
Assignee:
The Proctor & Gamble Company
Inventors:
Michael George Natchus, Biswanath De, Stanislaw Pikul, Neil Gregory Almstead, Roger Gunnard Bookland, Yetunde Olabisi Taiwo, Menyan Cheng
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: Neuroprotective agents are disclosed having the following structure:
wherein R1, R2, R3, R4 and R5 are as defined herein. Such compounds have utility in the treatment of conditions which benefit from administration of neuroprotective agents generally, including treatment of central and peripheral nervous condition as well as for promoting nerve cell differentiation. Methods of treating such conditions are also disclosed, as are pharmaceutical compositions containing one or more of the compounds of this invention.
Type:
Grant
Filed:
November 27, 2000
Date of Patent:
June 4, 2002
Assignee:
Nippon Kayaku Co., Ltd.
Inventors:
Moorthy S. S. Palanki, Shripad S. Bhagwat, Hiroshi Sato, Paul E. Erdman, Mary Doubleday
Abstract: This application relates to novel compounds of formula I (and their pharmaceutically acceptable salts), as defined herein, processes and intermediates for their preparation, pharmaceutical formulations comprising the novel compounds of formula I, and the use of defined compounds of formula I as thrombin inhibitors.
Type:
Grant
Filed:
January 21, 2000
Date of Patent:
May 21, 2002
Assignee:
Eli Lilly and Company
Inventors:
Nickolay Y Chirgadze, Michael L Denney, Matthew J Fisher, Robert J Foglesong, Richard W Harper, Mary G Johnson, Ho-Shen Lin, Michael P Lynch, Jefferson R McCowan, Shawn C Miller, Alan D Palkowitz, Michael E Richett, Daniel J Sall, Gerald F Smith, Kumiko Takeuchi, Minsheng Zhang
Abstract: Biaryls, e,g,. biphenyls, phenylpyridines, phenylfurans, phenylpyrroles, phenylthiophenes, bipyridines, pyridylfurans or pyridylpyrroles are prepared in high yields by coupling aromatics with an aromatic boric acid or boric ester in the presence of a palladaphosphacyclobutane catalyst.
Type:
Grant
Filed:
July 13, 2000
Date of Patent:
May 21, 2002
Assignee:
Clariant GmbH
Inventors:
Holger Geissler, Steffen Haber, Andreas Meudt, Frank Vollmueller, Stefan Scherer
Abstract: N-Benzoyl arylsulfonamides having the formula 1
Type:
Application
Filed:
August 24, 2001
Publication date:
May 9, 2002
Inventors:
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
Abstract: There is disclosed a genus of non-peptidyl compounds, wherein said compounds are VLA-4 inhibitors useful in treating inflammatory, autoimmune, and respiratory diseases, and wherein said compounds comprise a compound of Formula (1.0.
Type:
Application
Filed:
December 21, 2000
Publication date:
April 25, 2002
Inventors:
Allen J. Duplantier, Louis S. Chupak, Anthony J. Milici, Wan F. Lau
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:
February 28, 2001
Date of Patent:
April 23, 2002
Assignee:
COR Therapeutics, Inc.
Inventors:
Bing-Yan Zhu, Penglie Zhang, Lingyan Wang, Wenrong Huang, Erick A. Goldman, Wenhao Li, Jingmei Zuckett, Yonghong Song, Robert M. Scarborough
Abstract: Novel 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 disease and other diseases involving elevated levels of cytokines, as well as central nervous system (CNS) disorders, also is disclosed.
Type:
Grant
Filed:
December 7, 2000
Date of Patent:
April 23, 2002
Assignee:
ICOS Corporation
Inventors:
Timothy J. Martins, Kerry W. Fowler, Joshua Odingo, Laurence E. Burgess, Stephen T. Schlachter
Abstract: The present invention is directed to pyrrolidine compounds of the formula I:
(wherein R1, R2, R3, R4c, R4d, and R4f are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-3 and/or CCR-5.
Type:
Grant
Filed:
March 1, 2000
Date of Patent:
April 16, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Jianming Bao, Robert K. Baker, William H. Parsons, Kathleen Rupprecht
Abstract: The present invention relates to chalcone and chalcone derivatives and analogs which are useful as angiogenesis inhibitors. The present compounds, which are inexpensive to synthesize, exhibit unexpectedly good activity as angiogenesis inhibitors. The present invention also relates to the use of chalcone and its analogs as antitumor/anticancer agents and to treat a number of conditions or disease states in which angiogenesis is a factor, including angiongenic skin diseases such as psoriasis, acne, rosacea, warts, eczema, hemangiomas, lymphangiogenesis, among numerous others, as well as chronic inflammatory disease such as arthritis.
Type:
Application
Filed:
December 26, 2000
Publication date:
April 4, 2002
Inventors:
J. Phillip Bowen, Thomas Philip Robinson, Tedman Ehlers, David Goldsmith, Jack Arbiser
Abstract: The present invention is directed to pyrrolidine compounds of the formula I:
(wherein R1, R2, R3, R4c, R4d, and R4f are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-3 and/or CCR-5.
Type:
Grant
Filed:
March 1, 2000
Date of Patent:
March 26, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Robert K. Baker, William H. Parsons, Kathleen Rupprecht
Abstract: The present invention relates to 6-phenyl-pyridin-2-ylamine derivatives of the formula
wherein R1, R2, R3 and R4 are defined as in the specification, that exhibit activity as nitric oxide synthase (NOS) inhibitors, to pharmaceutical compositions containing them and to their use in the treatment and prevention of central nervous system and other disorders.
Abstract: The present invention relates to pharmaceutical compositions containing, as an active ingredient, at least one compound of formula:
in which R1 represents a radical —N(R4)R5, —N(R4)—CO—R5, —N(R4)—SO2R6 or one of its pharmaceutically acceptable salts, to the novel derivatives of formula (I), to their pharmaceutically acceptable salts and to their preparation.
Abstract: The present invention provides the compounds of the following formula (I):
and a method for inhibiting the reuptake of seretonin, antagonizing the 5-HT1A receptor and antagonizing the 5-HT2A receptor which comprises administering to a subject in need of such treatment an effective amount of formula (I).
Abstract: Dihydropyridine derivatives of the following formula, analogs thereof and pharmaceutically acceptable salts thereof have an activity of selectively inhibiting the action of N-type calcium channel. They are used as remedies for various diseases relating to the N-type calcium channel.
Abstract: Novel compounds that are potent and selective inhibitors of PIDE4, 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:
Grant
Filed:
November 17, 2000
Date of Patent:
February 19, 2002
Assignee:
ICOS Corporation
Inventors:
Kerry W. Fowler, Amy Oliver, Joshua Odingo
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:
Application
Filed:
February 28, 2001
Publication date:
January 3, 2002
Inventors:
Bing-Yan Zhu, Penglie Zhang, Lingyan Wang, Wenrong Huang, Erick A. Goldman, Wenhao Li, Jingmei Zuckett, Yonghong Song, Robert Scarborough
Abstract: The present invention relates to quinolinium- and pyridinium-based fluorescent dyes. The dyes are useful for staining proteins in solution, in gels and on solid supports. The dyes of the invention exhibit higher fluorescence emission than known compounds when bound to proteins and also exhibit improved contrast of fluorescence intensity between their protein-bound and unbound states.
Type:
Grant
Filed:
October 5, 1999
Date of Patent:
January 1, 2002
Assignee:
Oxford Glycosciences (UK) Ltd.
Inventors:
Mark William Pennington, David Ian Scopes, Michael Glen Orchard
Abstract: Described is a heterocycle-containing carboxylic acid derivative represented by the following formula (I):
wherein A represents, for example, a heteroaryl group which contains at least one nitrogen atom and may have a substituent, B represents, for example, a heteroarylene group, a —CONH— group or a group represented by the formula —CR6═CR7— in which R6 and R7 represents H, a lower alkyl group or the like, D represents an arylene group, a heteroarylene group or the like, n1 stands for 0 or 1, M represents, for example, a hydroxyl group or a lower alkoxy group; or a physiologically acceptable salt thereof. As a retinoic-related compound replacing retinoic acid, it permits the provision of a preventive and/or therapeutic for various diseases.
Abstract: A racemate, diastereoisomer and optical isomer of a compound of formula (I):
wherein B is H, a C6 or C10 aryl, C7-16 aralkyl; Het or (lower alkyl)-Het, all of which may be optionally substituted with C1-6 alkyl; C1-6 alkoxy; C1-6 alkanoyl; hydroxy; hydroxyalkyl; halo; haloalkyl; nitro; cyano; cyanoalkyl; amino optionally substituted with C1-6 alkyl; amido; or (lower alkyl)amide; or
B is an acyl derivative of formula R4—C(O)—; a carboxyl derivative of formula R4—O—C(O)—; an amide derivative of formula R4—N(R5)—C(O)—; a thioamide derivative of formula R4—N(R5)—C(S)—; or a sulfonyl of formula R4—SO2; R5 is H or C1-6 alkyl; and
Y is H or C1-6 alkyl;
R3 is C1-8 alkyl, C3-7 cycloalkyl, or C4-10 alkylcycloalkyl, all optionally substituted with hydroxy, C1-6 alkoxy, C1-6 thioalkyl, amido, (lower alkyl)amido, C6 or C10 aryl, or C7-16 aralkyl;
R2 is CH2—R20, NH—R20, O—R20 or S—R20, wherein R20 is a satu