Additional Nitrogen Containing Hetero Ring Attached Directly Or Indirectly To The Seven-membered Hetero Ring By Nonionic Bonding Patents (Class 514/211.15)
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Publication number: 20040157825Abstract: The present invention relates to the use of quinolone carboxylic acid formulations in the treatment of ocular and periocular infections. The present invention also relates to sustained release compositions comprising specific quinolone carboxylic acid compounds. The invention also relates to quinolone carboxylic acid compositions and methods of preparing the same.Type: ApplicationFiled: February 2, 2004Publication date: August 12, 2004Inventors: Samir Roy, Santosh Kumar Chandrasekaran, Katsumi Imamori, Takemitsu Asaoka, Akihiro Shibata, Masami Takahashi, Lyle M. Bowman
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Publication number: 20040132716Abstract: CGRP antagonists of theformula 1Type: ApplicationFiled: October 15, 2003Publication date: July 8, 2004Applicant: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Klaus Rudolf, Stephan Georg Mueller, Dirk Stenkamp, Philipp Lustenberger, Alexander Dreyer, Eckhart Bauer, Marcus Schindler, Kirsten Arndt, Henri Doods
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Publication number: 20040132715Abstract: A method to treat allergic rhinitis is disclosed in which patients are administered certain indolyl compounds.Type: ApplicationFiled: September 5, 2003Publication date: July 8, 2004Inventors: Paul J. Dunford, James P. Edwards, Lars Karlsson, Wai-Ping Leung, Robin L. Thurmond, Jianmei Wei
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Patent number: 6743817Abstract: Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof wherein R, Ar, A, n, R1 and R2 are defined herein. These compounds are highly selective agonists, antagonists or inverse agonists for GABAA brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAA brain receptors and are therefore useful in the diagnosis and treatment of anxiety, depression, Down Syndrome, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are also disclosed.Type: GrantFiled: September 6, 2001Date of Patent: June 1, 2004Assignee: Neurogen CorporationInventors: George Maynard, LingHong Xie, Stanislaw Rachwal
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Patent number: 6727247Abstract: A compound of formula I and a method of treatment of diseases, related to modulation of the adenosine A2 receptor system comprising administering a compound of formula to a person in need of such treatment.Type: GrantFiled: December 3, 2002Date of Patent: April 27, 2004Assignee: Hoffman-La Roche Inc.Inventors: Alexander Flohr, Roland Jakob-Roetne, Roger David Norcross, Claus Riemer
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Publication number: 20040077626Abstract: The present invention describes difluororthioacetamide oxazolidinones as novel antibacterial agents, and antimicrobial combination therapies for combating infective diseases caused by gram-positive and gram-negative bacteria.Type: ApplicationFiled: June 16, 2003Publication date: April 22, 2004Inventors: Jackson Boling Hester, Wade J. Adams, Jeffrey Charles Stevens, Mikhail Fedor Gordeev, Upinder Singh, Carole Scott
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Publication number: 20040063686Abstract: Compounds of formula (I) in which: each A is independently hydrogen, C1-6alkyl optionally substituted by hydroxyl, C1-6alkoxy, C1-6alkenyl or C1-6acyl group or a halogen atom or hydroxyl, CN or CF3 group; R3 is hydrogen, methyl or ethyl; R4 is an optionally substituted aromatic carbocyclic or heterocyclic ring; Z is an O or S atom, or an NH or CH2 group, or a single bond, at the 3 or 4 position of R4 relative to the carbonyl group; R5 is an optionally substituted aromatic carbocyclic or heterocyclic ring, or an optionally substituted, saturated or unsaturated, carbocyclic or heterocyclic ring; and Q is (a) Where X, Y, R1 and R2 are as defined in claim 1; are antagonists of a human 11CBy receptor.Type: ApplicationFiled: September 30, 2003Publication date: April 1, 2004Inventors: Christopher Norbert Johnson, Martin Jones, Catherine Anne O'Toole, Geoffrey Stemp, Kevin Michael Thewlis, David Witty
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Patent number: 6713478Abstract: This invention provides compounds of Formula (I): wherein R1 and R2 are independent substituents or are fused to form spirocyclic rings; R3, RC, and R4 are as defined herein; and R5 is a substituted benzene ring or a substituted five or six membered heterocyclic ring having in its backbone 1, 2, or 3 heteroatoms including O, S, SO, SO2 or NR6; or pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions and methods using the compounds as antagonists of the progesterone receptor.Type: GrantFiled: March 12, 2003Date of Patent: March 30, 2004Assignees: Wyeth, Ligand Pharmaceuticals, Inc.Inventors: Puwen Zhang, Eugene A. Terefenko, Andrew Fensome, Jay E. Wrobel, Horace Fletcher, III, Lin Zhi, Todd K. Jones, James P. Edwards, Christopher M. Tegley
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Patent number: 6713472Abstract: A compound which is a chymase inhibitor and which is represented by a formula [I] and salts thereof. In the formula [I], X is R6—(A2)n—N, R1 and R2 are H, alkyl, cycloalkyl or aryl, R3 and R4 are H, alkyl, cycloalkyl, aryl or aromatic heterocycle, R5 is H, alkyl, cycloalkyl, aryl or —A3—A4—R7, R6 is H, alkyl, cycloalkyl, OH, alkoxy, aryl, aryloxy or an aromatic heterocycle, R7 is H, alkyl, OH, alkoxy, aryl, aryloxy, amino, alkylamino, arylamino, an aromatic heterocycle or a nonaromatic heterocycle, A1 is alkylene, A2 is carbonyl or sulfonyl, A3 is alkylene, A4 is carbonyl or oxalyl and n is o or 1.Type: GrantFiled: January 18, 2002Date of Patent: March 30, 2004Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Kazuo Nishimura, Masakazu Ban, Ken-ichi Fujimura, Naoyuki Kobayashi, Masanori Hori, Eiko Matsumoto
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Publication number: 20040034011Abstract: Compounds of formula (I′), wherein A, R1 to R3 and t are as defined in the disclosure, exhibit COMT enzyme inhibiting activity so that they are useful as COMT inhibitors.Type: ApplicationFiled: July 9, 2003Publication date: February 19, 2004Inventors: Reijo Bckstrm, Jarmo Pystynen, Timo Lotta, Martti Ovaska, Jyrki Taskinen
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Publication number: 20040029859Abstract: Compounds of formula (I): 1Type: ApplicationFiled: March 12, 2003Publication date: February 12, 2004Applicant: Pfizer Inc.Inventors: Julian Blagg, Michael Jonathan Fray, Mark Llewellyn Lewis, John Paul Mathias, Mark Henryk Stefaniak, Alan Stobie
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Publication number: 20040029861Abstract: The invention relates to the use of pharmacologically valuable pyridyl alkane, pyridyl alkene and/or pyridyl alkine acid amides according to general formula (I) in the treatment of tumors or for immunosuppression.Type: ApplicationFiled: July 30, 2002Publication date: February 12, 2004Applicant: Klinge Pharma GmbHInventors: Elfi Biedermann, Max Hasmann, Roland Loser, Benno Rattel, Friedemann Reiter, Barbara Schein, Klaus Seibel, Klaus Vogt
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Publication number: 20040014741Abstract: The present invention provides non-steroidal compounds of Formula I, including prodrugs and pharmaceutically acceptable salts thereof, which are selective modulators (e.g., agonists, partial agonists and antagonists) of a steroid receptor, specifically, the glucocorticoid receptor. The present invention also provides pharmaceutical compositions containing these compounds and methods for using these compounds to treat animals requiring glucocorticoid receptor agonist or antagonist therapy. Glucocorticoid receptor modulators are useful to treat diseases, such as obesity, diabetes, inflammation and others as described below. The present invention also provides processes for preparing these compounds.Type: ApplicationFiled: October 26, 2001Publication date: January 22, 2004Inventors: Kevin K. Liu, Bradley P. Morgan, Ralph P. Robinson
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Publication number: 20040009967Abstract: The invention relates to new pyridyl alkane acid amides according to general formula (I) as well as methods for their production, medicaments containing these compounds as well as their medical use, especially in the treatment of tumors or for immunosuppression.Type: ApplicationFiled: July 30, 2002Publication date: January 15, 2004Applicant: Klinge Pharma GmbHInventors: Elfi Biedermann, Max Hasmann, Roland Loser, Benno Rattel, Friedemann Reiter, Barbara Schein, Klaus Seibel, Klaus Vogt
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Publication number: 20030236247Abstract: Compounds having the formula 1Type: ApplicationFiled: March 21, 2003Publication date: December 25, 2003Inventors: Steven W. Elmore, Cheol-Min Park, Xilu Wang
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Patent number: 6656932Abstract: Selective MMP-13 inhibitors are benzo thiadiazines of the Formula or a pharmaceutically acceptable salt thereof, wherein R2 is hydrogen or alkyl; R1 and R3 include hydrogen, alkyl, and aryl, with the proviso that R3 is not (CH2)m biphenyl or (CH2)m substituted biphenyl; X is O or NH, n is 0, 1, or 2. The compounds of Formula I, or a pharmaceutically acceptable salt thereof, is useful for treating diseases mediated by an MMP-13 enzyme, including diseases selected from osteoarthritis, rheumatoid arthritis, cancer, inflammation, and heart failure.Type: GrantFiled: February 13, 2002Date of Patent: December 2, 2003Assignee: Warner-Lambert CompanyInventors: Joseph Armand Picard, Michael William Wilson
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Publication number: 20030220319Abstract: This invention relates to compounds which are alpha-1 receptor agonists, preferably alpha-1A/L receptor agonists, and which are represented by Formula I: 1Type: ApplicationFiled: January 31, 2003Publication date: November 27, 2003Inventors: Robert Greenhouse, Saul Jaime-Figueroa, Lubica Raptova
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Publication number: 20030207842Abstract: Novel compounds having activity as non-covalent inhibitors of urokinase and having activity in reducing or inhibiting blood vessel formation are provided. These compounds have at a group having a guanidino moiety or derivative thereof. These compounds are useful in vitro for monitoring plasminogen activator levels and in vivo in treatment of conditions which are ameliorated by inhibition of or decreased activity of urokinase and in treating pathologic conditions wherein blood vessel formation is related to a pathologic condition.Type: ApplicationFiled: December 4, 2002Publication date: November 6, 2003Inventors: Amir P. Tamiz, L. Josue Alfaro-Lopez, Odile Esther Levy, Joseph Edward Semple
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Patent number: 6642242Abstract: The invention provides compounds of formula (I), wherein R1 represents C1-4 alkoxy optionally substituted by one or more fluorine atoms; R2 represents H or C1-6 alkoxy optionally substituted by one or more fluorine atoms; R3 represents one or more groups independently selected from H, halogen, C1-4 alkoxy and CF3; in addition, R2 and one R3 group may together represent —OCH2—, the methylene group being attached to the ortho-position of the pendant phenyl ring; R4 represents a 4-, 5- or 6-membered heterocyclic ring containing 1 or 2 heteroatoms selected from N, O and S, the ring being optionally fused to a benzene ring or a 5- or 6-membered heterocyclic ring containing 1 or 2 heteroatoms selected from N, O and S, the ring system as a whole being optionally substituted; X represents CH or N; and L is absent or represents a cyclic group or an open chain group; and pharmaceutically acceptable salts thereof.Type: GrantFiled: March 19, 2001Date of Patent: November 4, 2003Assignee: Pfizer Inc.Inventors: Alan John Collis, David Nathan Abraham Fox, Julie Newman
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Patent number: 6635637Abstract: Cyclic oxyguanidine compounds, including compounds of Formulae I and II: wherein R1, R3-R6, R21-R26, L, Y, Z, and A are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formulae I and II. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity.Type: GrantFiled: August 2, 2001Date of Patent: October 21, 2003Assignee: Dimensional Pharmaceuticals, Inc.Inventors: Aihua Wang, Tianbao Lu, Bruce Edward Tomczuk, Richard M. Soll, John Curtis Spurlino, Roger Francis Bone
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Publication number: 20030191110Abstract: The present invention relates to methods for modulating the cholesterol biosynthetic pathway. The level of cholesterol in the body is linked to numerous pathological states. The methods of the present invention alter the transcription levels of genes involved in the cholesterol biosynthesis. The methods of the present invention can used for treating diseases mediated by the cholesterol biosynthetic pathway.Type: ApplicationFiled: November 1, 2002Publication date: October 9, 2003Inventors: Martyn Botfield, Fiona McDonald, Joern Kraetzschmar, Bernhard Lindenthal, Bertold Kreft
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Patent number: 6630475Abstract: Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, cycloalkenyl, or heteroaryl; X is alkylene or —C(O)CH2—; Y is —N(R2)CH2CH2N(R)3)—, —OCH2CH2N(R2)—, —O—, —S—, —CH2S—, —(CH2)2—NH—, or optionally substituted m and n are 2-3, and Q is nitrogen or optionally substituted carbon; and Z is optionally substituted phenyl, phenylalkyl or heteroaryl, diphenylmethyl, R6—C(O)—, R6—SO2—, R6—OC(O)—, R7—N(R8)—C(O)—, R7—N(R8)—C(S)—, phenyl-CH(OH)—, or phenyl-C(═NOR2)—; or when Q is CH, phenylamino or pyridylamino; or Z and Y together are substituted piperidinyl or substituted phenyl; and R2, R3, R6, R7, and R8 are as defined in the specification are disclosed, their use in the treatment of ParkinsoType: GrantFiled: May 24, 2001Date of Patent: October 7, 2003Assignee: Schering CorporationInventors: Bernard R. Neustadt, Neil Lindo, William J. Greenlee, Deen Tulshian, Lisa S. Silverman, Yan Xia, Craig D. Boyle, Samuel Chackalamannil
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Publication number: 20030186960Abstract: The present invention relates to cyclized amino acid derivatives for treating or preventing neuronal damage associated with neurological diseases. The invention also provides compositions comprising the compounds of the present invention and methods of utilizing those compositions for treating or preventing neuronal damage.Type: ApplicationFiled: January 3, 2002Publication date: October 2, 2003Inventors: David Lauffer, Brian Ledford
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Publication number: 20030176415Abstract: The invention relates to novel 1,2,3,4-tetrahydroisochinoline derivatives of formula (I) and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as orexin receptor antagonists.Type: ApplicationFiled: February 24, 2003Publication date: September 18, 2003Inventors: Hamed Aissaoui, Michael Cappi, Martine Clozel, Walter Fischli, Ralf Koberstein
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Publication number: 20030176694Abstract: Compounds, compositions and methods are provided that are useful in the treatment and/or prevention of a condition or disorder mediated by a G-protein coupled receptor. In particular, the compounds of the invention are useful in the treatment and/or prevention of eating disorders, obesity, anxiety disorders and mood disorders.Type: ApplicationFiled: November 6, 2002Publication date: September 18, 2003Inventors: Xiaoqi Chen, Pingchen Fan, Juan Jaen, Leping Li, Mike Lizarzaburu, Jeffrey Thomas Mihalic, Stephen Joseph Shuttleworth
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Publication number: 20030171354Abstract: The present invention relates to compounds of formula I which are antagonists of gonadotropin releasing hormone (GnRH) activity. The invention also relates to pharmaceutical formulations, the use of a compound of the present invention in the manufacture of a medicament, a method of therapeutic treatment using such a compound and processes for producing the compounds.Type: ApplicationFiled: August 21, 2002Publication date: September 11, 2003Applicant: AstraZeneca ABInventors: Michael Wardleworth, Alexander Graham Dossetter, Christopher Thomas Halsall
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Patent number: 6617329Abstract: Compounds of the formula having an inhibitory effect on signal transduction mediated by tyrosine kinases, their use in the treatment of diseases, especially tumoral diseases and diseases of the lungs and air-ways, and the preparation thereof.Type: GrantFiled: August 23, 2001Date of Patent: September 9, 2003Assignee: Boehringer Ingelheim Pharma KGInventors: Frank Himmelsbach, Elke Langkopf, Birgit Jung, Stefan Blech, Flavio Solca
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Publication number: 20030166633Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof wherein R1, R2 and R3 represent various functional groups, and one of X1 and X2 is N and the other is NR10; and their use as pharmaceuticals.Type: ApplicationFiled: October 29, 2002Publication date: September 4, 2003Inventors: Laramie Mary Gaster, Michael Stewart Hadley, John David Harling, Frank Peter Harrington, Jag Paul Heer, Thomas Daniel Heightman, Andrew Hele Payne
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Patent number: 6610697Abstract: This invention relates to a series of imidazopyrimidines of Formula I, and pharmaceutical compositions containing them. The compounds of the invention inhibit the production of a number of inflammatory cytokines and are useful in the treatment and prevention of diseases associated with the overproduction thereof.Type: GrantFiled: October 27, 2000Date of Patent: August 26, 2003Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: John H. Dodd, James R. Henry, Kenneth C. Rupert
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Publication number: 20030158179Abstract: Compounds of formula I 1Type: ApplicationFiled: September 19, 2002Publication date: August 21, 2003Inventors: Michael G. Klug, Patrizio Mattei, Werner Mueller, Werner Neidhart, Matthias Heinrich Nettekoven, Philippe Pflieger, Jean-Marc Plancher
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Patent number: 6608048Abstract: This invention provides compounds of Formula (I), where A″, Z, X and n are defined herein, or a pharmaceutically acceptable salt thereof which are useful as antineoplastic agents and in the treatment of polycystic kidney disease.Type: GrantFiled: March 28, 2001Date of Patent: August 19, 2003Assignee: Wyeth HoldingsInventors: Hwei-Ru Tsou, Elsebe Geraldine Overbeek-Klumpers, Allan Wissner
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Patent number: 6608070Abstract: This invention provides a compound of the following formula: or the pharmaceutically acceptable salts thereof wherein Z is OH, C1-6 alkoxy, —NR2R3 or heterocycle; Q is selected from the following: (a) an optionally substituted phenyl, (b) an optionally substituted 6-membered monocyclic aromatic group containing one, two, three or four nitrogen atom(s), (c) an optionally substituted 5-membered monocyclic aromatic group containing one heteroatom selected from O, S and N and optionally containing one, two or three nitrogen atom(s) in addition to said heteroatom, (d) an optionally substituted C3-7 cycloalkyl and (e) an optionally substituted benzo-fuzed heterocycle; R1 is hydrogen, C1-4 alkyl or halo; R2 and R3 are independently hydrogen, OH, C1-4 alkoxy, C1-4 alkyl or C1-4 alkyl substituted with halo, OH, C1-4 alkoxy or CN; X is independently selected from H, halo, C1-4 alkyl, halo-substituted C1-4 alkyl, OH, C1-4 alkoxy, halo-substituted C1-4 alkoxy, C1-4 alkylthio, NO2, NH2, di-(C1-4 alType: GrantFiled: July 28, 1999Date of Patent: August 19, 2003Inventors: Kazunari Nakao, Rodney William Stevens, Kiyoshi Kawamura, Chikara Uchida, Hiroki Koike, Stephane Caron
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Publication number: 20030149023Abstract: Compounds of general formula (I) 1Type: ApplicationFiled: August 19, 2002Publication date: August 7, 2003Applicant: AstraZeneca Canada Inc.Inventors: Daniel Delorme, Edward Roberts, Zhongyong Wei
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Publication number: 20030144262Abstract: This invention relates to a series of N-heterocyclyl hydrazides of Formula I, 1Type: ApplicationFiled: October 4, 2002Publication date: July 31, 2003Inventors: Zhihua Sui, Mark Macielag, James Lanter
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Publication number: 20030144263Abstract: Compounds of the formula (I), or a pharmaceutically-acceptable salt, or an in-vivo-hydrolysable ester thereof, 1Type: ApplicationFiled: January 9, 2003Publication date: July 31, 2003Applicant: Syngenta LimitedInventor: Michael Barry Gravestock
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Publication number: 20030134840Abstract: The invention provides compounds of general formula 1Type: ApplicationFiled: January 9, 2003Publication date: July 17, 2003Applicant: AstraZeneca AB, a Sweden corporationInventors: Andrew Baxter, Stephen Brough, Nicholas Kindon, Thomas Mclnally, Bryan Roberts, Stephen Thom
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Publication number: 20030130258Abstract: The present invention relates to compounds with the formula (I) 1Type: ApplicationFiled: November 22, 2002Publication date: July 10, 2003Inventors: Guido Kurz, Marianne Nilsson, Jerk Vallgarda, Meredith Williams
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Publication number: 20030130259Abstract: Compounds of formula I, 1Type: ApplicationFiled: December 13, 2002Publication date: July 10, 2003Inventor: David Nathan Abraham Fox
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Publication number: 20030114436Abstract: 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: ApplicationFiled: November 5, 2002Publication date: June 19, 2003Inventors: Brian M. Aquila, Gregory D. Cuny, James R. Hauske, Liming Shao, Xinhe Wu
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Patent number: 6579868Abstract: The present invention provides a preventive or therapeutic agent of a new type for diabetes mellitus and diabetic complications on the basis of an adenosine A2 receptor antagonistic action. A purine compound represented by the formula (I), its pharmacologically acceptable salt or hydrates thereof has an adenosine A2 receptor antagonistic action and is useful for prevention or therapy of diabetes mellitus and diabetic complications. In addition, adenosine A2 receptor antagonists having different structures from those of the compounds described above, for example KW6002, are also effective for prevention or therapy of diabetes mellitus and diabetic complications. In the formula, W is —CH2CH2—, —CH═CH— or —C≡C—; R1 is: (in the formula, X is hydrogen atom, hydroxyl group, a lower alkyl group, a lower alkoxy group, etc.Type: GrantFiled: July 5, 2000Date of Patent: June 17, 2003Assignee: Eisai Co., Ltd.Inventors: Osamu Asano, Hitoshi Harada, Yorihisa Hoshino, Seiji Yoshikawa, Takashi Inoue, Tatsuo Horizoe, Nobuyuki Yasuda, Kaya Nagata, Junsaku Nagaoka, Manabu Murakami, Seiichi Kobayashi
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Patent number: 6566362Abstract: Benzo[f]naphthyridine derivatives of formula (I): benzo[f]naphthyridine derivatives and benzo[f]naphthyridine esters of formula (IVa): aminoquinoline derivatives of formula (X): processes for preparing such compounds; and compositions comprising them.Type: GrantFiled: December 31, 2001Date of Patent: May 20, 2003Assignee: Aventis Pharma S.A.Inventors: Jean-François Desconclois, Arielle Genevois-Borella, Philippe Girard, Michel Kryvenko, Marc Pierre Lavergne, Jean-Luc Malleron, Guy Picaut, Michel Tabart, Sylvie Wentzler
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Patent number: 6559155Abstract: Pyrimidones of formula (I) are inhibitors of the enzyme LpPLA2 and thereof use in treating inter alia atherosclerosis, in which: R1 is COOH or a salt thereof, COOR10, CONR11R12, CN or CH2OH; R2 is a mono- or bicyclic aromatic ring system or a mono- or bicyclic heteroaromatic ring system; R3 is C1-20alkyl, C3-6cycloalkyl, C3-6cycloalkylC1-5alkyl, C1-10alkoxyC1-10alkyl, or an aromatic or heteroaromatic ring system; W is SO2 or a bond; X is O or S; and Y is a group of the formula A1—A2—A3 in which A1 and A3 each represent a bond or a straight chain or branched alkylene group, said alkylene group(s) containing a total of 1 to 10 carbon atoms and A2 represents a bond or O, S, SO, SO2, CO, C═CH2, CONH, NHCO, CR15R16, CH═CH or C═C, providing that when A2 is O, S, SO, SO2 or CONH, A3 contains at least two carbon atoms linking the A2 group and the CH2 group in formula (I).Type: GrantFiled: February 21, 2001Date of Patent: May 6, 2003Assignee: SmithKline Beecham p.l.c.Inventors: Colin Andrew Leach, Stephen Allan Smith
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Publication number: 20030078252Abstract: The invention provides compounds of formula 1 1Type: ApplicationFiled: May 13, 2002Publication date: April 24, 2003Applicant: Pfizer Inc.Inventors: Mark A. Sanner, Chris J. Helal, Christopher B. Cooper
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Publication number: 20030073682Abstract: The present application describes novel substituted aryl hydroxamic acids of formula I: 1Type: ApplicationFiled: April 3, 2002Publication date: April 17, 2003Inventors: Matthew E. Voss, Carl P. Decicco, Ruth R. Wexler
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Publication number: 20030055037Abstract: Benzimidazole and indole derivatives that act as selective modulators of CRF 1 receptors are provided. These compounds are useful in the treatment of a number of CNS and periphereal disorders, particularly stress, anxiety, depression, cardiovascular disorders, and eating disorders. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided.Type: ApplicationFiled: October 5, 2001Publication date: March 20, 2003Inventors: Stephane DeLombaert, Ping Ge, Raymond F. Horvath, Taeyoung Yoon
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Publication number: 20030027790Abstract: There is provided a pharmaceutical preservative free composition suitable for topical administration to an eye, the composition comprising (a) an oxazolidinone antimicrobial drug, for example linezolid, in a therapeutically or prophylactically effective drug concentration that is above the practical limit of solubility of the drug in a substantially isotonic aqueous solution at a physiologically compatible pH, and (b) a pharmaceutically acceptable cyclodextrin compound in a concentration sufficient to maintain the drug-in solution at such a drug concentration. The composition is particularly useful for the treatment and/or prevention of eye infections due to gram positive bacteria.Type: ApplicationFiled: February 22, 2002Publication date: February 6, 2003Inventors: Satish K. Singh, Lisa A. Adams, Paramita Bandyopadhyay, Syed Hasan, Leslie C. Hawley, Sandra M. Sims
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Publication number: 20030018022Abstract: 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: ApplicationFiled: May 22, 2002Publication date: January 23, 2003Applicant: Tularik Inc.Inventors: Tassie Collins, Hossen Mahmud, Jonathan Houze, Alan Xi Huang, Julio C. Medina, Xuemei Wang, Feng Xu, Qingge Xu, Liusheng Zhu
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Patent number: 6509334Abstract: This invention provides compounds of Formula (I): wherein R1 and R2 may be single substituents or fused to form spirocyclic or hetero-spirocyclic rings; R3 is H, OH, NH2, C1 to C6 alkyl, substituted C1 to C6 alkyl, C3 to C6 alkenyl, substituted C1 to C6 alkenyl, alkynyl, or substituted alkynyl, CORC; RC is H, C1 to C3 alkyl, substituted C1 to C3 alkyl, aryl, substituted aryl, C1 to C3 alkoxy, substituted C1 to C3 alkoxy, C1 to C3 aminoalkyl, or substituted C1 to C3 aminoalkyl; R4 is H, halogen, CN, NO2, C1 to C6 alkyl, substituted C1 to C6 alkyl, alkynyl, or substituted alkynyl, C1 to C6 alkoxy, substituted C1 to C6 alkoxy, amino, C1 to C6 aminoalkyl, or substituted C1 to C6 aminoalkyl; and R5 is selected from a trisubstituted benzene ring of a five or six membered ring with 1, 2, or 3 heteroatoms from the group including O, S, SO, SO2 or NR6 and containing one or two independent substituents from the group including H, halogen, CN, N02, amino, and C1 to C3 alkyl, C1 to C3 alkoxy, C1 to C3 aType: GrantFiled: April 19, 2000Date of Patent: January 21, 2003Assignees: American Home Products Corporation, Ligand Pharmaceuticals, Inc.Inventors: Puwen Zhang, Eugene A. Terefenko, Andrew Fensome, Jay E. Wrobel, Horace Fletcher, III, Lin Zhi, Todd K. Jones, James P. Edwards, Christopher M. Tegley
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Publication number: 20020187193Abstract: The present invention relates to the use of quinolone carboxylic acid formulations in the treatment of ocular and periocular infections. The present invention also relates to sustained release compositions comprising specific quinolone carboxylic acid compounds. The invention also relates to quinolone carboxylic acid compositions and methods of preparing the same.Type: ApplicationFiled: April 25, 2001Publication date: December 12, 2002Inventors: Samir Roy, Santosh Kumar Chandrasekaran, Katsumi Imamori, Takemitsu Asaoka, Akihiro Shibata, Masami Takahashi, Lyle M. Bowman
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Publication number: 20020182255Abstract: The present invention relates to the use of quinolone carboxylic acid formulations in the treatment of ocular and periocular infections. The present invention also relates to sustained release compositions comprising specific quinolone carboxylic acid compounds. The invention also relates to quinolone carboxylic acid compositions and methods of preparing the same.Type: ApplicationFiled: April 22, 2002Publication date: December 5, 2002Inventors: Samir Roy, Santosh Kumar Chandrasekaran, Katsumi Imamori, Takemitsu Asaoka, Akihiro Shibata, Masami Takahashi, Lyle M. Bowman