Chalcogen In The Hetero Ring Patents (Class 540/488)
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Patent number: 6815463Abstract: Laulimalide compounds, intermediates thereto and methods for their preparation, and methods for their use in the treatment of diseases characterized by cellular hyperproliferation.Type: GrantFiled: February 10, 2003Date of Patent: November 9, 2004Assignee: Kosan Biosciences, Inc.Inventors: Gary Ashley, Brian Metcalf
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Publication number: 20040220175Abstract: The present invention relates to (pyrido/thieno)-[f]-oxazepine-5-one derivatives having the general Formula I wherein R1, R2 and R3 are independently H or (C1-4)alkyl; Ar represents a fused thiophene or pyridine ring optionally substituted with one or more substituents selected from (C1-4)alkyl, (C1-4)alkyloxy, (C1-4)alkyloxy(C1-4)alkyl, CF3, halogen, nitro, cyano, NR4R5, NR4COR6, and CONR4R5; R4 and R5 are independently H or (C1-4)-alkyl; or R4 and R5 form together with the nitrogen atom to which they are bound a 5-or 6-membered saturated heterocyclic ring, optionally containing a further heteroatom selected from O, S or NR6; R6 is (C1-4)alkyl; A represents the residue of a 4-7 membered saturated heterocyclic ring, optionally containing an oxygen atom, the ring being optionally substituted with 1-3 substituents selected from (C1-4)alkyl, (C1-4)-alkyloxy, hydroxy, halogen and oxo; or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: June 14, 2004Publication date: November 4, 2004Inventors: Simon James Anthony Grove, Julia Adam-Worall, Minggiang Zhang, Robert Gilfillan
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Patent number: 6806267Abstract: The present invention relates to pyrrolobenzoxazepines, pyrrolobenzthiazepines and related compounds having the ability to induce apoptosis, to pharmaceutical compositions comprising these compounds and to their use as anti-tumour agents.Type: GrantFiled: February 16, 2000Date of Patent: October 19, 2004Assignees: The Universita'di Siena, The Provost, Fellows and Scholars of the College of the Holy and Undivided Trinity of Queen Elizabeth Near DublinInventors: David Clive Williams, Daniela M. Zisterer, Vito Nacci, Giuseppe Campiani
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Publication number: 20040186091Abstract: A compound of formula (I), 1Type: ApplicationFiled: February 18, 2004Publication date: September 23, 2004Applicant: Pfizer IncInventors: Justin Stephen Bryans, Patrick Stephen Johnson, Thomas Ryckmans, Alan Stobie
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Publication number: 20040171605Abstract: The present invention relates to benzoxazepine derivative having the general formula I, wherein X represents CO or SO2; R1, R2, R3 and R4 are independently selected from H, (C1-4)alkyl, (C1-4)alkyloxy, (C1-4)alkyloxy(C1-4)alkyl, halogen, nitro, cyano, NR8R9, NR8COR10, and CONR8R9, R5, R6 and R7 are independently H or (C1-4)alkyl; R8 and R9 are independently H or (C1-4)alkyl; or R8 and R9 form together with the nitrogen atom to which they are bound a 5- or 6-membered saturated heterocyclic ring, optionally containing a further heteroatom selected from O, S or NR11; R10 is (C1-4)alkyl; R11 is (C1-4)alkyl; A represents the residue of a 4-7 membered saturated heterocyclic ring, optionally containing an oxygen atom, the ring being optionally substituted with 1-3 substituents selected from (C1-4)alkyl, (C1-4)alkyloxy, hydroxy, halogen and oxo; or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: December 11, 2003Publication date: September 2, 2004Inventors: Simon James Anthony Grove, Mingqiang Zhang
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Patent number: 6767907Abstract: 4-Aryl-1-(indanmethyl, dihydrobenzofuranmethyl or dihydrobenzothiophenemethyl)piperidine, -tetrahydropyridine or -piperazine compounds of general formula (I), wherein one of X and Y is CH2 and the other one is CH2, O or S; Z is N, C, CH or COH; Ar is an optionally substituted aryl group; R1 is hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, acyl, thioacyl, alkylsulfonyl, trifluoromethylsulfonyl, arylsulfonyl, a group R9VCO— where V is O or S and R9 is alkyl or aryl, or a group R10R11NCO— or R10R11NCS— wherein R10 and R11 are hydrogen, alkyl or aryl, or R10 and R11 are linked to form a ring; R2 is hydrogen, alkyl, cykcloalkyl or cycloalkylalkyl; or R1 and R2 are linked to form a ring; R3-R5 are hydrogen, halogen, alkyl, alkylcarbonyl, phenylcarbonyl, alkoxy, alkylthio, hydroxy, alkylsulfonyl, cyano, trifluoromethyl, cycloalkyl, cycloalkylalkyl or nitro; R6 and R7 are hydrogen or alkyl or they are linked to constitute 3-7 membered ring; R8 is hydrogen or alkyl; have effects at cType: GrantFiled: April 14, 2000Date of Patent: July 27, 2004Assignee: H. Lundbeck A/SInventors: Jens Kristian Perregaard, John Willie Stenberg, Bitten Hansen
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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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Patent number: 6759404Abstract: Novel cyclic malonamides having the formula (I): and their pharmaceutical compositions. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A&bgr;-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein.Type: GrantFiled: April 3, 2001Date of Patent: July 6, 2004Inventors: Richard E. Olson, Michael G. Yang
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Publication number: 20040077553Abstract: The present invention provides prodrugs of GABA analogs, pharmaceutical compositions of prodrugs of GABA analogs and methods for making prodrugs of GABA analogs. The present invention also provides methods for using prodrugs of GABA analogs and methods for using pharmaceutical compositions of prodrugs of GABA analogs for treating or preventing common diseases and/or disorders.Type: ApplicationFiled: December 6, 2002Publication date: April 22, 2004Inventors: Mark A. Gallop, Kenneth C. Cundy, Cindy X. Zhou, Fayang G. Qiu, Fenmei Yao, Jia-Ning Xiang, Ian R. Ollmann
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Patent number: 6686349Abstract: The invention relates to novel tetracyclic pyrroloquinolone derivatives of the formula (I) or (II): wherein all variables are as herein defined, pharmaceutical compositions containing the compounds and their use for the treatment of sexual dysfunction.Type: GrantFiled: November 12, 2002Date of Patent: February 3, 2004Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Weiqin Jiang, Zhihua Sui
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Patent number: 6686350Abstract: The present invention relates to novel compounds that are useful for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. This invention also relates to pharmaceutical formulations comprising these compounds and methods of using them for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. The compounds and pharmaceutical compositions of this invention can be used as therapeutic or prophylactic agents. They are particularly well-suited for treatment of many inflammatory and autoimmune diseases.Type: GrantFiled: January 25, 1999Date of Patent: February 3, 2004Assignee: Biogen, Inc.Inventors: Zhongli Zheng, Carol L. Ensinger, Steven P. Adams
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Publication number: 20040009966Abstract: The present invention relates to novel compounds, compositions comprising said compounds, and uses thereof, said compounds having the formula: 1Type: ApplicationFiled: June 9, 2003Publication date: January 15, 2004Applicant: The Procter & Gamble CompanyInventors: John August Wos, Yili Wang, Kofi Abeka Oppong, Steven Victor O'Neil, Michael Christopher Laufersweiler, David Lindsey Soper, Biswanath De, Thomas Prosser Demuth
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Patent number: 6670389Abstract: Laulimalide compounds, intermediates thereto and methods for their preparation, and methods for their use in the treatment of diseases characterized by cellular hyperproliferation.Type: GrantFiled: February 8, 2002Date of Patent: December 30, 2003Assignee: Kosan Biosciences, Inc.Inventors: Gary Ashley, Brian Metcalf
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Patent number: 6667301Abstract: This invention relates to compounds which are generally muscarinic M2/M3 receptor antagonists and which are represented by Formula I: wherein X, Y, and Z are O, S or NR5, and the other substituents are as defined in the specification; and prodrugs, individual isomers, racemic or non-racemic mixtures of isomers, and pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds and methods for their use as therapeutic agents.Type: GrantFiled: May 22, 2001Date of Patent: December 23, 2003Assignee: Syntex (U.S.A.) LLCInventors: Charles Alois Dvorak, Lawrence Emerson Fisher, Keena Lynn Green, Ralph New Harris, III, Hans Maag, Anthony Prince, David Bruce Repke, Russell Stephen Stabler
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Patent number: 6656911Abstract: 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.Type: GrantFiled: April 18, 2002Date of Patent: December 2, 2003Assignee: Cortech, Inc.Inventors: Albert Gyorkos, Lyle W Spruce
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Publication number: 20030220318Abstract: Specific phenylalanine derivatives or pharmaceutically acceptable. salts thereof have an antagonistic effect on the &agr;4 integrins and, therefore, are usable as therapeutic agents or preventive agents for diseases in which &agr;4 integrin-depending adhesion process participates in the pathology, such as inflammatory diseases, rheumatoid arthritis, inflammatory bowel diseases, systemic lupus erythematosus, multiple sclerosis, Sjögren's syndrome, asthma, psoriasis, allergy, diabetes, cardiovascular diseases, arterial sclerosis, restenosis, tumor proliferation, tumor metastasis and transplantation rejection.Type: ApplicationFiled: March 31, 2003Publication date: November 27, 2003Applicant: AJINOMOTO CO. INCInventors: Nobuyasu Suzuki, Toshihiko Yoshimura, Hiroyuki Izawa, Kazuyuki Sagi, Shingo Makino, Eiji Nakanishi, Masahiro Murata, Takashi Tsuji
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Patent number: 6645958Abstract: This invention relates to compounds which are generally muscarinic M2/M3 receptor antagonists and which are represented by Formula I: wherein X, Y, and Z are O, S, or NR4, and the other substituents are as defined in the specification; and prodrugs, individual isomers, racemic or non-racemic mixtures of isomers, and pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds and methods for their use as therapeutic agents.Type: GrantFiled: November 6, 2002Date of Patent: November 11, 2003Assignee: Syntex (U.S.A.) LLCInventors: Robert James Weikert, Ann Marie Madera, Russell Stephen Stabler
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Patent number: 6635759Abstract: The invention relates to a substituted 4-trifluoromethyl carbostyril according to formula (I) and is characterised in that the 4-trifluoromethyl carbostyril is provided with an absorption maximum between 350 and 420 nm and a luminescence maximum between 430 and 900 nm. The molecule can be substituted with groups that are useful for complexing metal ions and/or for binding the molecule to relevant groups of a target molecule or a solid supporting material. The carbostyril as described above can inter alia serve as an antenna molecule of a lanthanide complex. Said complexes can be templates and can be brought into contact with a directly bound or free colour molecule which absorbs in the rant of 580-710 nm. Luminescence effects and decay periods can be measured after the contact with a relevant analyte.Type: GrantFiled: December 31, 2001Date of Patent: October 21, 2003Inventors: Georg Uray, Karlheinz Niederreiter
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Publication number: 20030176398Abstract: The present invention provides prodrugs of GABA analogs, pharmaceutical compositions of prodrugs of GABA analogs and methods for making prodrugs of GABA analogs. The present invention also provides methods for using prodrugs of GABA analogs and methods for using pharmaceutical compositions of prodrugs of GABA analogs for treating or preventing common diseases and/or disorders.Type: ApplicationFiled: June 11, 2002Publication date: September 18, 2003Inventors: Mark A. Gallop, Kenneth C. Cundy, Cindy X. Zhou, Fayang G. Qiu, Fenmei Yao, Jia-Ning Xiang, Ian R. Ollmann
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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: 20030158170Abstract: A compound having the general formula (I) and methods of using such compounds for the treatment of diseases and pharmaceutical composition comprising such compounds.Type: ApplicationFiled: October 2, 2002Publication date: August 21, 2003Inventors: Jeffrey Scott Albert, Peter Bernstein, Cyrus Ohnmacht Jr, Keith Russell, Ashokkumar Bhikkappa Shenvi
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Publication number: 20030144268Abstract: The invention relates to novel tetracyclic pyrroloquinolone derivatives of the formula (I) or (II): 1Type: ApplicationFiled: November 12, 2002Publication date: July 31, 2003Inventors: Weiqin Jiang, Zhihua Sui
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Patent number: 6559141Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.Type: GrantFiled: July 27, 2001Date of Patent: May 6, 2003Assignees: Athena Neurosciences, Inc., Eli Lilly & CompanyInventors: Jing Wu, Jay S. Tung, Eugene D. Thorsett, Michael A. Pleiss, Jeffrey S. Nissen, R. Jeffrey Neitz, Lee H. Latimer, Varghese John, Stephen Freedman, Thomas C. Britton, James A. Audia, Jon K. Reel, Thomas E. Mabry, Bruce A. Dressman, Cynthia L. Cwi, James J. Droste, Steven S. Henry, Stacey L. McDaniel, William Leonard Scott, Russell D. Stucky, Warren J. Porter
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Publication number: 20030083495Abstract: An efficient process is described for the synthesis of 5, a key intermediate for the synthesis of the potent antitumor agents ecteinascidin 743 (1) and phthalascidin (2) from the readily available building blocks 3b and 4.Type: ApplicationFiled: August 7, 2002Publication date: May 1, 2003Applicant: President and Fellows of Harvard CollegeInventor: Elias J. Corey
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Publication number: 20030069204Abstract: The present invention relates to ester, ether and N-alkylcarbamoyl derivatives of compound (Ia) and pharmaceutically acceptable salts thereof. These compounds exhibit excellent antibacterial activity and are useful for the treatment or prevention of bacterial infections.Type: ApplicationFiled: March 12, 2002Publication date: April 10, 2003Applicant: SANKYO COMPANY LIMITEDInventors: Masatoshi Inukai, Masakatsu Kaneko, Toshio Takatsu, Hitoshi Hotoda, Masatoshi Arai, Shunichi Miyakoshi, Masaaki Kizuka, Yasumasa Ogawa
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Patent number: 6544978Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.Type: GrantFiled: July 27, 2001Date of Patent: April 8, 2003Assignees: Athena Neurosciences, Inc., Eli Lilly & CompanyInventors: Jing Wu, Jay S. Tung, Eugene D. Thorsett, Michael A. Pleiss, Jeffrey S. Nissen, R. Jeffrey Neitz, Lee H. Latimer, Varghese John, Stephen Freedman, Thomas C. Britton, James A. Audia, Jon K. Reel, Thomas E. Mabry, Bruce A. Dressman, Cynthia L. Cwi, James J. Droste, Steven S. Henry, Stacey L. McDaniel, William Leonard Scott, Russell D. Stucky, Warren J. Porter
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Patent number: 6541466Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.Type: GrantFiled: July 27, 2001Date of Patent: April 1, 2003Assignees: Athena Neurosciences, Inc., Eli Lilly & CompanyInventors: Jing Wu, Jay S. Tung, Eugene D. Thorsett, Michael A. Pleiss, Jeffrey S. Nissen, R. Jeffrey Neitz, Lee H. Latimer, Varghese John, Stephen Freedman, Thomas C. Britton, James A. Audia, Jon K. Reel, Thomas E. Mabry, Bruce A. Dressman, Cynthia L. Cwi, James J. Droste, Steven S. Henry, Stacey L. McDaniel, William Leonard Scott, Russell D. Stucky, Warren J. Porter
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Patent number: 6537987Abstract: This invention relates to certain benzoxazepinones and benzothiazepinones useful as hypocholesterolemic agents, hypotriglyceridemic agents, antiatherosclerosis agents, antifungal agents, anti-Alzheimer's agents or anti-acne agents.Type: GrantFiled: December 18, 1998Date of Patent: March 25, 2003Assignee: Pfizer Inc.Inventors: Ernest S. Hamanaka, Cheryl M. Hayward
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Patent number: 6503897Abstract: Compounds of formula (I) are antibacterial agents wherein: R3 and R4, taken together with the carbon atoms to which they are respectively attached, form an optionally substituted saturated carbocyclic or heterocyclic ring of 5 to 16 atoms, which may be benz-fused or fused to a second optionally substituted saturated carbocyclic or heterocyclic ring of 5 to 16 atoms; and R1 and R2 are as defined in the specification.Type: GrantFiled: August 22, 2001Date of Patent: January 7, 2003Assignee: British Biotech Pharmaceuticals Ltd.Inventors: Raymond Paul Beckett, Mark Whittaker, Zoe Marie Spavold
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Publication number: 20020183513Abstract: Compounds of formula I 1Type: ApplicationFiled: April 22, 2002Publication date: December 5, 2002Inventors: Adelbert Grossmann, Wolfgang von der Saal, Tim Sattelkau, Ulrich Tibes
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Patent number: 6489320Abstract: The present invention relates to benzoxazepinones of formula I: or stereoisomeric forms or mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HIV reverse transcriptase, and to pharmaceutical compositions and diagnostic kits comprising the same and methods of using the same for treating viral infection or as an assay standard or reagent.Type: GrantFiled: September 7, 2000Date of Patent: December 3, 2002Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Anthony J. Cocuzza, James D. Rodgers
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Patent number: 6472529Abstract: A compound of the formula: is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.Type: GrantFiled: April 18, 2001Date of Patent: October 29, 2002Assignee: Abbott LaboratoriesInventors: Hing Leung Sham, Daniel W. Norbeck, Xiaoqi Chen, David A. Betebenner, Dale J. Kempf, Thomas R. Herrin, Gondi N. Kumar, Stephen L. Condon, Arthur J. Cooper, Daniel A. Dickman, Steven M. Hannick, Lawrence Kolaczkowski, Patricia A. Oliver, Daniel J. Plata, Peter J. Stengel, Eric J. Stoner, Jieh-Heh J. Tien, Jih-Hua Liu, Ketan M. Patel
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Patent number: 6472384Abstract: The present invention relates to ester, ether and N-alkylcarbamoyl derivatives of compound (Ia) and pharmaceutically acceptable salts thereof. These compounds exhibit excellent antibacterial activity and are useful for the treatment or prevention of bacterial infections. (wherein R1 is a hydrogen atom or a methyl group; R2a is a hydrogen atom, a protecting group for a hydroxy group, or a methyl group; R3 is a hydrogen atom or a protecting group for a hydroxy group; R4a is a hydrogen atom, a hydroxy group or a protected hydroxy group; R5 is a hydrogen atom or a protecting group for a hydroxy group; and X is a methylene group or a sulfur atom). The invention also includes compounds which are related to the aforeidentified compounds.Type: GrantFiled: January 9, 2001Date of Patent: October 29, 2002Assignee: Sankyo Company, LimitedInventors: Masatoshi Inukai, Masakatsu Kaneko, Toshio Takatsu, Hitoshi Hotoda, Masatoshi Arai, Shunichi Miyakoshi, Masaaki Kizuka, Yasumasa Ogawa
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Patent number: 6468996Abstract: The present invention relates to compounds of the general formula (I) The compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).Type: GrantFiled: October 19, 1999Date of Patent: October 22, 2002Assignees: Novo Nordisk A/S, Dr. Reddy's Research FoundationInventors: Lone Jeppesen, Paul Stanley Bury, Per Sauerberg
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Patent number: 6458827Abstract: A method of modifying or altering the structure of a 1&agr;-hydroxylated vitamin D compound to increase its biological activity by altering the conformational equilibrium of the A-ring to favor a chair conformation that presents the 1&agr;-hydroxyl in the axial orientation. This is accomplished by either locking the A-ring chair conformation in a geometry having an axially orientated 1&agr;-hydroxyl, or by the addition of one or more substituents to the A-ring which interact with other substituents in the molecule or on the A-ring to provide a driving force to the A-ring to adopt a chair conformation which presents the 1&agr;-hydroxyl in the axial orientation.Type: GrantFiled: July 20, 2001Date of Patent: October 1, 2002Assignee: Wisconsin Alumni Research FoundationInventors: Hector F. DeLuca, Rafal R. Sicinski
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Patent number: 6452011Abstract: The present invention relates to a method for preparing piperidine derivative compounds by converting, with a piperidine compound, regioisomers having the formula: where Z is or and where m is 1 or 4-6; Q and Y are the same or different and are selected from the group consisting of O, S, and NR5; R6 and R7 are the same or different and are selected from the group consisting of hydrogen, an alkyl moiety, an aryl moiety, OR8, SR8, and NR8R9; X3 is halogen, OR15, SR15, NR15R16, OSO2R15, or NHSO2R15; R5, R8, R9, R15, and R16 are the same or different and are selected from the group consisting of hydrogen, an alkyl moiety, and an aryl moiety; and A is a substituent of its ring and is selected from the group consisting of hydrogen, halogens, alkyl, hydroxy, alkoxy, and other substituents.Type: GrantFiled: August 9, 2000Date of Patent: September 17, 2002Assignee: Albany Molecular Research, Inc.Inventors: Thomas E. D'Ambra, Garry M. Pilling
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Patent number: 6444824Abstract: The present invention relates to a method for preparing piperidine derivative compounds by converting, with a piperidine compound, regioisomers having the formula: where Z is and where m is 1 or 3-6; Q and Y are the same or different and are selected from the group consisting of O, S, and NR5; R6 and R7 are the same or different and are selected from the group consisting of hydrogen, an alkyl moiety, an aryl moiety, OR8, SR8, and NR8R9; and R5, R8, and R9 are the same or different and are selected from the group consisting of hyrogen, an alkyl moiety, and an aryl moiety.Type: GrantFiled: August 9, 2000Date of Patent: September 3, 2002Assignee: Albany Molecular Research, Inc.Inventors: Thomas E. D'Ambra, Garry M. Pilling
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Patent number: 6444809Abstract: Compounds of formula I wherein G, J, L, M, m and D have any of the meanings given in the specification, their N-oxides, and their pharmaceutically acceptable salts are nonpeptide antagonists of neurokinin A and useful for the treatment of asthma, etc. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.Type: GrantFiled: September 22, 2000Date of Patent: September 3, 2002Assignee: Zeneca LimitedInventor: Scott Carson Miller
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Publication number: 20020091116Abstract: Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.Type: ApplicationFiled: February 28, 2001Publication date: July 11, 2002Inventors: Bing-Yan Zhu, Zhaozhong Jon Jia, Wenrong Huang, Yonghong Song, James Kanter, Robert M. Scarborough
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Patent number: 6416922Abstract: The present invention related to an azomethine dye precursor represented by the following general formula (1) and the image-forming material and image-forming method using the azomethine dye precursor: wherein Ar represents an aryl group or a heterocyclic group which may each have a substituent; X represents a bivalent group linking a carbon atom and a nitrogen atom; and Cp represent a coupler residue which may or may not form a ring.Type: GrantFiled: January 29, 2001Date of Patent: July 9, 2002Assignee: Fuji Photo Film Co., Ltd.Inventors: Hiroshi Sato, Masatoshi Yumoto, Yoshimitsu Arai, Hirotaka Matsumoto
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Patent number: 6399598Abstract: The invention provides compounds of formula as described in the claims, or an optical isomer, diastereomer or enantiomer thereof, or a pharmaceutically-acceptacle salt, or biohydrolyzable amide, ester, or imide thereof are useful as inhibitors of metalloproteases. Also disclosed are pharmaceutical compositions and methods of treating diseases, disorders and conditions characterized by metalloprotease activity using these compounds or the pharmaceutical compositions containing them.Type: GrantFiled: March 1, 2000Date of Patent: June 4, 2002Assignee: The Procter & Gamble CompanyInventors: Stanislaw Pikul, Neil Gregory Almstead, Rimma Sandler Bradley, Kelly Lynn McDow-Dunham, Biswanath De, Michael George Natchus, Yetunde Olabisi Taiwo, Thomas Lee Cupps
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Publication number: 20020055499Abstract: Compounds of the formula (I) are disclosed which are dual fibrinogen receptor and vitronectin receptor antagonists and are useful in the treatment of atherosclerosis, in the prevention of restenosis and in the prevention of tumor metastasis and tumor growth: 1Type: ApplicationFiled: December 12, 2001Publication date: May 9, 2002Inventors: Dirk Heerding, James Martin Samanen
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Publication number: 20020049193Abstract: This invention relates to neurotrophic low molecular weight, small molecule N-linked sulfonamides of heterocyclic thioesters having an affinity for FKBP-type immunophilins, and their use as inhibitors of the enzyme activity associated with immunophilin proteins, particularly peptidyl-prolyl isomerase, or rotamase, enzyme activity.Type: ApplicationFiled: August 10, 2001Publication date: April 25, 2002Applicant: GPI NIL HOLDINGS, INC.Inventors: Gregory S. Hamilton, Jai-He Li, Wei Huang
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Publication number: 20020042411Abstract: A condensed thiophene compound of the formula (I) 1Type: ApplicationFiled: April 19, 2001Publication date: April 11, 2002Inventors: Koji Seio, Hiroshi Tanaka, Toshiyuki Kohara, Kenji Hashimoto, Masatake Fujimura, Hideki Horiuchi, Hiroshi Yasumatsu, Koreichi Kimura
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Publication number: 20020004501Abstract: This invention relates to compounds which are generally muscarinic M2/M3 receptor antagonists and which are represented by Formula I: 1Type: ApplicationFiled: May 22, 2001Publication date: January 10, 2002Inventors: Charles Alois Dvorak, Lawrence Emerson Fisher, Keena Lynn Green, Ralph New Harris, Hans Maag, Anthony Prince, David Bruce Repke, Russell Stephen Stabler
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Patent number: 6297232Abstract: The invention relates to triazolo[4,5-d]pyrimidin-3-yl derivatives which are useful in the treatment of platelet aggregation disorders.Type: GrantFiled: February 19, 1999Date of Patent: October 2, 2001Assignee: AstraZeneca ABInventors: Roger Victor Bonnert, Anthony Howard Ingall, Brian Springthorpe, Paul Andrew Willis
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Patent number: 6218394Abstract: 4-Aryl-1-(indanmethyl, dihydrobenzofuramethyl or dihydrobenzothiophenemethyl) piperidine, -tetrahydropyridine or -piperazine compounds of general formula (I) wherein one of X and Y is CH2, and the other one is CH2, O or S; Z is N, C, CH or COH; Ar is an optionally substituted aryl group; R1 is hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, acyl, thioacyl, alkylsulfonyl, trifluoromethylsulfonyl, arylsulfonyl, a group R9VCO— where V is O or S and R9 is alkyl or aryl, or a group R10R11NCO— or R10R11NCS— wherein R10 and R11 are hydrogen, alkyl or aryl, or R10 and R11 are linked to form a ring; R2 is hydrogen, alkyl, cycloalkyl or cycloalkylalkyl; or R1 and R2 are linked to form a ring; R3-R5 are hydrogen, halogen, alkyl, alkylcarbonyl, phenylcarbonyl, alkoxy, alkylthio, hydroxy, alkylsulfonyl, cyano, trifluoromethyl, cycloalkyl, cycloalkylalkyl or nitro; R6 and R7 are hydrogen or alkyl or they are linked to constitute a 3-7-membered ring; R8 is hydrogen or alkylType: GrantFiled: December 9, 1996Date of Patent: April 17, 2001Assignee: H. Lundbeck A/SInventors: Jens Kristian Perregaard, John Willie Stenberg, Bitten Hansen
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Patent number: 6147071Abstract: Novel compounds of the following general formula or salts thereof. ##STR1## wherein Ring M is a heterocyclic ring having --N.dbd.CC<, --CO--N< or --CS--N< as the partial structure --X . . . . . Y<; R.sup.a and R.sup.b are bonded to each other to form Ring A, or they are the same or different and represent, independently, a hydrogen atom or a substituent on the Ring M; Ring A and Ring B represent, independently, an optionally substituted homocyclic or heterocyclic ring, and at least one of them is optionally substituted heterocyclic ring; Ring C is optionally substituted homocyclic or heterocyclic ring; Ring Z is an optionally substituted ring; and n represents an integer of from 1 to 6, or a salt thereof, which has an excellent tachykinin receptor antagonistic effect, and their production, and pharmaceutical compositions.Type: GrantFiled: June 1, 1998Date of Patent: November 14, 2000Assignee: Takeda Chemical Industries, Ltd.Inventors: Hideaki Natsugari, Takenori Ishimaru, Takayuki Doi, Yoshinori Ikeura, Chiharu Kimura
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Patent number: 6140320Abstract: The present invention relates to benzoxazepinones of formula I: ##STR1## or stereoisomeric forms or mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HIV reverse transcriptase, and to pharmaceutical compositions and diagnostic kits comprising the same and methods of using the same for treating viral infection or as an assay standard or reagent.Type: GrantFiled: September 1, 1998Date of Patent: October 31, 2000Assignee: Dupont Pharmaceuticals CompanyInventors: Anthony J. Cocuzza, James D. Rodgers
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Patent number: 6124279Abstract: Compounds of formula I ##STR1## wherein G, J, L, M, m and D have any of the meanings given in the specification, their N-oxides, and their pharmaceutically acceptable salts are nonpeptide antagonists of neurokinin A and useful for the treatment of asthma, etc. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.Type: GrantFiled: June 18, 1999Date of Patent: September 26, 2000Assignee: Zeneca LimitedInventor: Scott Carson Miller