Abstract: The present invention is directed to multibinding compounds which are &bgr;2 adrenergic receptor agonists and are therefore useful in the treatment and prevention of respiratory diseases such asthma, bronchitis, and the like. They are also useful in the treatment of nervous system injury and premature labor.
Abstract: The invention relates to novel benzimidazole derivatives with general formula I, whereby radicals R1, R2, R3, A, B, Y and Z have the meanings that are indicated in the description and the claims, the use of these compounds for the production of a pharmaceutical agent for treatment and prevention of diseases associated with microglia activation as well as pharmaceutical preparations that contain these compounds.
Type:
Application
Filed:
July 9, 2002
Publication date:
July 3, 2003
Inventors:
Thorsten Blume, Wolfgang Halfbrodt, Joachim Kuhnke, Ursula Monning, Herbert Schneider
Abstract: Compound of formula (I)
wherein:
R1 is hydrogen or C1-C6-alkyl optionally substituted by C3-C6-cycloylalkyl;
R2 and R3 together with the nitrogen form a saturated or unsaturated 5- or 6-membered heterocyclic ring optionally containing nitrogen or oxygen as an additional heteroatom, wherein the heterocyclic ring thereof is substituted by a group selected from phenyl, benzyl, and diphenylmethyl, each optionally mono- or di-substituted by one or two groups selected from CF3, C1-C4-alkyl, C1-C4-alkoxy, phenyl, benzyl, halogen, and OH, or
R2 and R3 together with the nitrogen form a saturated or unsaturated 5- or 6-membered heterocyclic ring optionally containing nitrogen or oxygen as an additional heteroatom, the heterocyclic ring thereof linked via a single bond, a methylene-bridge, or spiro-connected to another saturated or unsaturated heterocyclic group containing one or two heteroatoms selected from oxygen and nitrogen, the heterocyclic group being optionally mono- or di-substituted by a g
Abstract: The invention relates to the polymorph A of flibanserin, to a technical process for the preparation thereof, as well as to the use thereof for preparing medicaments.
Type:
Application
Filed:
August 1, 2002
Publication date:
June 26, 2003
Applicant:
Boehringer Ingelheim International GmbH
Inventors:
Carlo Bombarda, Enrica Dubini, Antoine Ezhaya
Abstract: The present invention concerns compounds of formula
the N-oxide forms, the salts, the quaternary amines and stereochemically isomeric forms thereof, wherein
D represents a tetrahydrofuran or dioxolane ring substituted with aryl and azolmethyl; —A—B— represents an optionally substituted bivalent radical of formula —N═CH—, —CH═N—, —CH═CH—, —CH2—CH2; Alk represents C1-6alkanediyl; Y represents optionally substituted C1-6alkanediyl; R1 and R2 represent hydrogen, C1-6alkyl or arylC1-6alkyl; or R1 and R2 may be taken together to form an optionally substituted heterocyclic radical selected from morpholinyl, pyrrolidinyl, piperidinyl, homopiperidinyl, piperazinyl or phthalimid-1-yl; aryl represents phenyl, naphthalenyl, 1,2,3,4-tetrahydro-naphthalenyl, indenyl or indanyl; each of said aryl groups may optionally be substituted; having broad-spectrum antifungal activity; their preparation, compositions containing them an
Type:
Grant
Filed:
February 4, 2002
Date of Patent:
June 24, 2003
Assignee:
Janssen Pharmacuetica N.V.
Inventors:
Lieven Meerpoel, Leo Jacobus Jozef Backx
Abstract: One aspect of the present invention relates to novel heterocyclic compounds comprising urea functionality. A second aspect of the present invention relates to the use of the novel heterocyclic compounds comprising urea functionality as ligands for various cellular receptors, including opioid receptors, other G-protein-coupled receptors and ion channels. An additional aspect of the present invention relates to the use of the novel heterocyclic compounds comprising urea functionality as analgesics.
Type:
Application
Filed:
November 5, 2002
Publication date:
June 19, 2003
Inventors:
Brian M. Aquila, Gregory D. Cuny, James R. Hauske, Liming Shao, Xinhe Wu
Abstract: This invention relates to a transition metal mediated process for the preparation of optionally substituted 2-amino-benzoxazoles and or 2-amino-benzimidazoles, which are useful as therapeutic agents or as intermediates in the synthesis of therapeutic agents.
Type:
Application
Filed:
September 20, 2002
Publication date:
June 12, 2003
Inventors:
Neil Wishart, Alena Rudolph, Kurt Ritter
Abstract: Compounds of general formula (I), wherein R1 selected from phenyl, pyridinyl, thiophenyl, furanyl, imidazolyl, and triazolyl; where each R1 phenyl ring and R1 heteroaromatic ring may optionally and independently be further substituted by 1, 2 or 3 substituents selected from straight and branched C1-C6 alkyl, NO2, CF3, C1-C6 alkoxy, chloro, fluoro, bromo, and iodo.
Type:
Application
Filed:
October 21, 2002
Publication date:
June 5, 2003
Inventors:
William Brown, Christopher Walpole, Niklas Plobeck
Abstract: The invention concerns oligobenzimidazole derivatives capable of combining with nucleic acids and their uses including for transferring in vitro, in vivo, or ex vivo nucleic acids into cells or for visual display of nucleic acids administered by fluorescence.
Type:
Application
Filed:
May 6, 2002
Publication date:
June 5, 2003
Inventors:
Daniel Scherman, Michel Bessodes, Bruno Pitard, Javier Soto, Gerardo Byk
Abstract: The invention comprises substituted indoleoxoacetic piperazine derivatives of general Formula I,
compositions thereof and their use as antiviral agents, and particularly for treating HIV infection.
Type:
Grant
Filed:
December 19, 2001
Date of Patent:
June 3, 2003
Assignee:
Bristol-Myers Sqibb Company
Inventors:
Owen B. Wallace, Tao Wang, Kap-Sun Yeung, Bradley C. Pearce, Nicholas A. Meanwell, Zhilei Qiu, Haiquan Fang, Qiufen May Xue, Zhiwei Yin
Abstract: This invention is directed to acyl piperazine derivatives of the following formula (Id):
wherein R1b, R3, R4, R5, R6 and R10 are described herein. These derivatives are useful as anti-inflammatory agents. This invention is also directed to pharmaceutical compositions containing the derivatives, and methods of using the derivatives to treat inflammatory disorders in humans.
Type:
Grant
Filed:
November 16, 2000
Date of Patent:
June 3, 2003
Assignee:
Schering Aktiengesellschaft
Inventors:
John G. Bauman, Brad O. Buckman, Ameen F. Ghannam, Joseph E. Hesselgesser, Richard Horuk, Imadul Islam, Meina Liang, Karen B. May, Sean D. Monahan, Michael M. Morrissey, Howard P. Ng, Kenneth J. Shaw, Guo Ping Wei, Wei Xu, Zuchun Zhao, Wei Zheng
Abstract: Bis-sulfonamido hydroxyethylamino compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to retroviral protease inhibiting compounds of the formula:
or a pharmaceutically acceptable salt, prodrug or ester thereof, wherein the variables are as defined herein.
Type:
Grant
Filed:
February 19, 2002
Date of Patent:
May 27, 2003
Assignee:
G. D. Searle & Co.
Inventors:
John N. Freskos, Daniel P. Getman, John J. Talley, James A. Sikorski
Abstract: Novel arylsulfonamide ether compounds and pharmaceutical compositions thereof are described. The use of the novel arylsulfonamide ether compounds and pharmaceutical compositions thereof as inhibitors of interleukin-1&bgr; converting enzyme and other cysteine proteases in the ICE family is also decribed. In addition, methods of treating stroke, inflammatory diseases, septic shock, repurfusion injury, Alzheimer's disease, and shigellosis using a compound of the invention or a pharmaceutical composition thereof are described.
Type:
Application
Filed:
May 10, 2002
Publication date:
May 22, 2003
Inventors:
James Knobelsdorf, Sheryl Hays, Charles J. Stankovic, Kimberly S. Para, Michael K. Connolly, Paul Galatsis, William Harter, Aurash B. Shahripour, Mark Stephen Plummer, Beth Lunney, Bernd Janssen, Jay Bradford Fell
Abstract: The invention provides compounds of general formula (I)
wherein R1, R2, R3, R4, A, Q, U, V, W, X, Y and n are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy, especially for the treatment of chemokine receptor related diseases and conditions.
Type:
Grant
Filed:
September 8, 2000
Date of Patent:
May 20, 2003
Assignee:
AstraZeneca UK Limited
Inventors:
Andrew J G Baxter, Stephen J Brough, Thomas McInally
Abstract: The invention relates to therapeutic benzamide compounds of formula (I)
wherein A, X, Z, R1, Y, R2, R3, are as defined herein, and physiologically acceptable salts, solvates or derivatives thereof. The present invention also provides pharmaceutical compositions, processes for the preparation of compounds of formula (I) and their use in the treatment of conditions mediated by ApoB-100 regulation.
Abstract: Use of a compound of formula (I):
wherein
X is optionally substituted aminoalkyl, optionally substituted alkylene or an interactive group;
Y and Z may be the same or different and are selected from N, O, S and C(R′) wherein R′ is hydrogen, optionally substituted alkyl or optionally substituted alkenyl;
---- is a double bond unless the attached Y or Z group is O or S in which case it is a single bond;
and R1 to R11 may be the same or different and are selected from hydrogen, a sterically hindering group and an electron donating group; or any two of R1 to R11, Y, Z, NH and R′ may together with the carbon atoms to which they are attached form an optionally substituted ring which may contain heteroatoms, provided that at least one of R1 to R11 is an electron donating group and that when X is NCH3, Y and Z are N and R1, R2 and R4 to R11 are hydrogen, then R3 is not OH or OCH2CH3; and salts thereof, pharmaceutically acceptable derivatives thereof, pro-drugs thereof and/or tau
Type:
Grant
Filed:
August 14, 2000
Date of Patent:
April 15, 2003
Assignee:
Peter MacCallum Cancer Institute
Inventors:
Roger Francis Martin, David Patterson Kelly, Jonathon Michael White
Abstract: This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with indoleoxoacetyl piperazine derivatives. These compounds possess unique antiviral activity, whether used alone or in combination with other antivirals, antiinfectives, immunomodulators or HIV entry inhibitors. More particularly, the present invention relates to the treatment of HIV and AIDS.
Type:
Application
Filed:
December 19, 2001
Publication date:
April 10, 2003
Inventors:
Owen B. Wallace, Tao Wang, Kap-Sun Yeung, Bradley C. Pearce, Nicholas A. Meanwell, Zhilei Qiu, Haiquan Fang, Qiufen May Xue, Zhiwei Yin
Abstract: Disclosed are multibinding compounds which are &bgr;2 adrenergic receptor agonists and are useful in the treatment and prevention of respiratory diseases such as asthma, bronchitis. They are also useful in the treatment of nervous system injury and premature labor.
Abstract: The present invention relates to certain substituted oxadiazole, thiadiazoles and triazole peptoids which are useful as inhibitors of serine proteases. Compounds of the invention are useful for treating, for example, adult respiratory distress syndrome, septic shock, and myocardial ischemia-reperfusion injury.
Abstract: The invention relates to novel benzimidazole derivatives with general formula I, whereby radicals R1, R2, R3, A, B and Y have the meanings that are indicated in the description and the claims, the use of these compounds for the production of a pharmaceutical agent for treating and for preventing diseases that are associated with microglia activation, as well as pharmaceutical preparations that contain these compounds.
Type:
Application
Filed:
July 5, 2002
Publication date:
March 20, 2003
Applicant:
Schering AG
Inventors:
Thorsten Blume, Wolfgang Halfbrodt, Joachim Kuhnke, Ursula Moenning, Herbert Schneider, Bernd Elger
Abstract: The present invention relates to novel benzimidazole derivatives, pharmaceutical composition containing these compounds, and methods of treatment therewith. The compounds of the invention are useful in the treatment of central nervous system diseases and disorders, which are responsive to modulation of the GABA receptor complex, and in particular for inducing and maintaining anesthesia, sedation and muscle relaxation, as well as for combating febrile convulsions in children. The compounds of the invention may also be used by veterinarians.
Abstract: The present invention is directed to peptidomimetic macrocyclic compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.
Type:
Grant
Filed:
April 6, 2001
Date of Patent:
March 18, 2003
Assignee:
Merck & Co., Inc.
Inventors:
Diem N. Nguyen, Craig A. Stump, Theresa M. Williams
Abstract: This invention relates to novel phenyl oxazoles, thiazoles, oxazolines, oxadiazoles and benzoxazoles useful as neuro-protective agents.
Type:
Application
Filed:
September 3, 2002
Publication date:
March 13, 2003
Inventors:
Jill Ann Panetta, John Kevin Shadle, Lawrence Joseph Heinz, Michael LeRoy Phillips, John Robert Rizzo, Benjamin Alan Anderson, John Allan Rieck, David Lee Varie
Abstract: A compound of formula (I)
wherein:
R1 is C1-C6-alkyl substituted by a group selected from OH, C1-C6-alkoxy, —OCONHC1-C6-alkyl, —OCONHC1-C6-alkyl, —NHSO2C1-C6-alkyl, and —NHCOC1-C6-alkyl, or
R1 is C1-C6-alkyl substituted by a saturated or unsaturated 5- or 6-membered heterocycle containing one or two heteroatoms selected from the group consisting of nitrogen and oxygen, the heterocycle optionally substituted by a group selected from C1-C4-alkyl, halogen, and benzyl;
R2 and R3 together with the nitrogen form a saturated or unsaturated 5- or 6-membered heterocyclic ring optionally containing nitrogen or oxygen as an additional heteroatom, the heterocyclic ring thereof substituted by a group selected from phenyl, benzyl, and diphenylmethyl, each of these groups optionally mono- or di-substituted by one or two groups selected from CF3, C1-C4-alkyl, C1-C4-alkoxy, phenyl, benzyl, halogen, and OH, or
R2 and R3 together with the nitrogen form a saturated or unsaturated 5-
Abstract: The present invention relates to compounds of the formula (I):
wherein R1a, R1b, R2, R3, R4, R5, X and n are defined herein. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migraine, emesis and postherpetic neuralgia.
Type:
Grant
Filed:
September 4, 2001
Date of Patent:
February 11, 2003
Assignee:
Merck Sharp & Dohme Ltd.
Inventors:
Kevin Tyler Chapman, Kevin Dinnell, Jason Matthew Elliott, Gregory John Hollingworth, Steven Michael Hutchins, Duncan Edward Shaw, Christopher Alan Willoughby
Abstract: The invention relates to piperazine derivatives, to processes for their preparation, to pharmaceutical compositions containing them, and to their medical use. The novel compounds are antagonists of tachykinins, including substance P and other neurokinins.
Type:
Application
Filed:
July 3, 2002
Publication date:
February 6, 2003
Inventors:
Giuseppe Alvaro, Romano Di Fabio, Riccardo Giovannini, Giuseppe Guercio, Yves St-Denis, Antonella Ursini
Abstract: A class of pyrazole derivatives is described for use in treating p38 kinase mediated disorders. Compounds of particular interest are defined by Formula IA
wherein R1, R2, R3 and R4 are as described in the specification.
Type:
Grant
Filed:
November 20, 1998
Date of Patent:
February 4, 2003
Assignee:
G.D. Searle & Company
Inventors:
Ashok Anantanarayan, Michael Clare, Paul W. Collins, Joyce Zuowu Crich, Rajesh Devraj, Daniel L. Flynn, Lifeng Geng, Matthew J. Graneto, Cathleen E. Hanau, Gunnar J. Hanson, Susan J. Hartmann, Michael Hepperle, He Huang, Francis J. Koszyk, Shuyuan Liao, Suzanne Metz, Richard A. Partis, Thao D. Perry, Shashidhar N. Rao, Shaun Raj Selness, Michael S. South, Michael A. Stealey, John Jeffrey Talley, Michael L. Vazquez, Richard M. Weier, Xiangdong Xu, Ish K. Khanna, Yi Yu
Abstract: The present invention relates to a novel series of 4-phenylpiperazines, 4-phenylpiperidines and 4-phenyl-1,2,3,6-tetrahydropyridines compounds of general formula (I)
wherein A is alkylene, alkenylene, alkynylene, and C3-7 cycloalkylene; R1 is a C3-10 alkyl, alkenyl, or alkynyl group, cycloalk(en)yl, cycloalk(en)yl-alk(en/yn)yl, trifluoromethylsulfonyl, or alkylsulfonyl, R2-R5 are optional substituents; R9 and R10 are hydrogen, alkyl or together form an ethylene or propylene bridge; W is O or S; V is O, S, CR6R7, or NR8 wherein R6, R7, and R8 are hydrogen or alkyl, alkenyl, cycloalkyl, cycloalkylalkyl, optionally substituted arylalkyl or aryl, or R6 and R7 constitute a 3-7 membered spiro ring; Z is —(CH2)m—, m being 2 or 3 or Z is —CH═CH—; X is N, C or CH; show effects on central serotonin 5-HT1A and dopamine D2 receptors. Thus the novel compounds are useful in the treatment of certain psychic and neurologic disorders, in particular psychosis.
Type:
Grant
Filed:
December 9, 1996
Date of Patent:
February 4, 2003
Assignee:
H. Lundbeck A/S
Inventors:
Jens Kristian Perregaard, Ejner Knud Moltzen
Abstract: A method for treating diseases in which tryptase inhibitors may be of thereapeutic value, which comprises the administration of a thereapeutic amount of a compound of the formula
The invention also comprises novel compounds of the formula (I). Exemplary is 2-[2-(4-amidinophenyl)ethyl]-1-methyl-benzimidazol-5-yl-carboxylic acid-N-(pyridin-3-yl-methyl)-N-methyl-amide-hydrochloride.
Type:
Grant
Filed:
August 8, 2000
Date of Patent:
January 28, 2003
Assignee:
Boehringer Ingelheim Pharma KG
Inventors:
Ralf Anderskewitz, Christine Braun, Hans Briem, Bernd Disse, Christoph Hoenke, Hans Michael Jennewein, Georg Speck
Abstract: The present invention relates to a novel pyrrole derivative which shows an inhibitory activity against farnesyl transferase or pharmaceutically acceptable salts or isomers thereof; to a process for preparation of said compound; and to a pharmaceutical composition such as anti-cancer composition, etc. comprising said compound as an active ingredient together with pharmaceutically acceptable carrier.
Type:
Grant
Filed:
October 11, 2001
Date of Patent:
January 28, 2003
Assignee:
LG Life Sciences, Ltd.
Inventors:
Jong-Sung Koh, Hyun-Il Lee, You-Seung Shin, Hak-Joong Kim, Jin-Ho Lee, Jong-Hyun Kim, Hyun-Ho Chung, Shin-Wu Jeong, Tae-Saeng Choi, Jung-Kwon Yoo, Chung-Mi Kim, Kwi-Hwa Kim, Sun-Hwa Lee, Sang-Kyun Lee
Abstract: Compounds, compositions and methods are provided that are useful in the treatment of chemokine receptor-mediated conditions and diseases. In particular, the invention provides compounds which modulate CCR4 function or a CCR4-mediated response. The subject compounds and compositions are useful for the treatment or prevention of inflammatory conditions and diseases.
Type:
Application
Filed:
May 22, 2002
Publication date:
January 23, 2003
Applicant:
Tularik Inc.
Inventors:
Tassie Collins, Hossen Mahmud, Jonathan Houze, Alan Xi Huang, Julio C. Medina, Xuemei Wang, Feng Xu, Qingge Xu, Liusheng Zhu
Abstract: The present invention concerns antiviral compounds, their compositions, and use in the treatment of viral infections. More particularly, the invention provides benzimidazolone derivatives for the treatment of respiratory syncytial virus infection.
Type:
Grant
Filed:
September 14, 2001
Date of Patent:
January 14, 2003
Assignee:
Bristol-Myers Squibb Company
Inventors:
Kuo-Long Yu, Rita Civiello, Keith Combrink, Hatice Belgin Gulgeze, Bradley C. Pearce, Xiangdong Wang, Nicholas A. Meanwell, Yi Zhang
Abstract: Chemical compounds of the formula
as well as pharmaceutical compositions containing them and methods for their use in the treatment of disorders and diseases responsive to modulation of the GABAA receptor complex of the central nervous system, such disorders and diseases including anxiety, sleep disorders, anesthesia, memory disorders, and epilepsy and other convulsive disorders.
Abstract: Succinoylamino hydroxyethylamino sulfonyl urea derivatives are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
Type:
Application
Filed:
December 11, 2001
Publication date:
December 26, 2002
Applicant:
G.D. Searle & Co.
Inventors:
Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
Abstract: A compound of the Formula (I):
wherein Z, R1, R, and Ar2 are as defined in the specification. This invention also relates to sulfonamide compounds of the Formula (I) that are inhibitors of procollagen C-proteinase, pharmaceutical compositions containing them, methods for their use, and methods for preparing the compounds.
Type:
Grant
Filed:
December 22, 1999
Date of Patent:
December 10, 2002
Assignee:
Syntex (U.S.A.) LLC
Inventors:
Roland Joseph Billledeau, Chris Allen Broka, Jeffrey Allen Campbell, Jian Jeffrey Chen, Sharon Marie Dankwardt, Nancy Delaet, Leslie Ann Robinson, Keith Adrian Murray Walker
Abstract: The middle value selection circuit includes three high value selection circuits and one low value selection circuit. Each high value selection circuit consists of a pair of first NPN transistors and a first constant current circuit. The emitter of each first NPN transistor of the high value selection circuit is connected to the first constant current circuit and the base of the second NPN transistor of the low value selection circuit. The base of this second NPN transistor is connected to the second constant current circuit and to an output terminal. The collector of the second NPN transistor is connected to its base. The first constant current circuit produces a current whichis twice the output current of the second constant current circuit. Two analog signals having mutually different combination among three input analog signals are applied to the NPN transistors of one high value selection circuit.