The Additional Hetero Ring Is A Cyclo In A Polycyclo Ring System Patents (Class 548/364.4)
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Patent number: 6630506Abstract: Acyl guanidines are provided which are sodium/proton exchange (NHE) inhibitors which have the structure wherein n is 0 to 4; X is a bond, O, S, SO, SO2, CO, or NR7; Y is a bond, O, S, SO, SO2, CO, or NR7′ wherein at least one of X and Y is other than a bond; and R1, R2, R3, R4, R5, R6, R7 and Ra, Rb, Rc, Rd are as defined herein, and are useful as antianginal, cardioprotective agents, antiischemic agents, and agents for peripheral vascular disease including intermittent claudication. In addition, a method is provided for preventing or treating angina pectoris, cardiac dysfunction, myocardial necrosis, arrhythmia, peripheral vascular diseases (PVD), including peripheral atherosclerotic disease (PAD), including intermittent claudication, Raynaud's diseases, and LeRiches Syndrome, pain, parethesia or discomfort in the lower limb and gluteal regions produced by vascular (e.g.Type: GrantFiled: April 21, 2000Date of Patent: October 7, 2003Assignee: Bristol-Myers Squibb Co.Inventors: Sundeep Dugar, Steven V. O'Neil
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Publication number: 20030186975Abstract: Compounds of formula (I′) wherein the two OH— substituents in the phenyl moiety are in a position ortho to one another and R1 in a position ortho to one of the hydroxy groups; and X, R1 to R6 are as defined in claims, exhibit COMT enzyme inhibiting activity so that they are useful as COMT inhibitors.Type: ApplicationFiled: March 31, 2003Publication date: October 2, 2003Inventors: Jarmo Pystynen, Martti Ovaska, Jukka Vidgren, Timo Lotta, Marjo Yliperttula-Ikonen
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Publication number: 20030181447Abstract: This invention is directed to 3-(diarylmethylene)-8-azabicyclo[3.2.1]octane derivatives useful as &dgr;-opioid or &mgr;-opioid receptor modulators. Depending on their agonist or antagonist effect, the compounds are useful analgesics, immunosuppressants, antiinflammatory agents, agents for the treatment of neurological and psychiatric conditions, medicaments for drug and alcohol abuse, agents for treating gastritis and diarrhea, cardiovascular agents and agents for the treatment of respiratory diseases.Type: ApplicationFiled: February 7, 2003Publication date: September 25, 2003Inventors: Robert E. Boyd, John R. Carson, Steven J. Coats, Lou Anne Neilson, Philip M. Pitis, Wu-Nan Wu
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Publication number: 20030166932Abstract: Compounds of the formula 1Type: ApplicationFiled: January 4, 2002Publication date: September 4, 2003Inventors: Richard L. Beard, Thong Vu, Diana F. Colon, Vidyasagar Vuligonda, Roshantha A. Chandraratna
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Patent number: 6610737Abstract: Novel non-psychotropic cannabinoids are disclosed and pharmaceutical compositions comprising these novel compounds are described for preventing neurotoxicity, neuroinflammation, immune or inflammatory disorders comprising as active ingredient the stereospecific (+) enantiomer, having (3S,4S) configuration of &Dgr;6 tetrahydrocannabinol type compounds. The compositions are particularly effective in alleviating and even preventing neurotoxicity due to acute injuries to the central nervous system, including mechanical trauma, compromised or reduced blood supply as may occur in cardiac arrest or stroke, or poisonings. They are also effective in the treatment of certain inflammatory disorders and chronic degenerative diseases characterized by neuronal loss and chronic pain including neuropathic pain.Type: GrantFiled: November 26, 2002Date of Patent: August 26, 2003Assignee: Pharmos CorporationInventors: Aaron Garzon, George Fink
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Patent number: 6610687Abstract: The invention relates to benzofuranylsulfonates of the general formula (I), their preparation and their use for the treatment of inflammation.Type: GrantFiled: February 25, 2002Date of Patent: August 26, 2003Assignee: Bayer AktiengesellschaftInventors: Gabriele Bräunlich, Mazen Es-Sayed, Rüdiger Fischer, Burkhard Fugmann, Rolf Henning, Stephan Schneider, Michael Sperzel, Karl-Heinz Schlemmer, Graham Sturton, Mary F. Fitzgerald, Barbara Briggs, Arnel Concepcion, William Bullock
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Patent number: 6600050Abstract: Diaminopyrazole derivatives of the general Formula (I) or their physiological tolerated, water-soluble salts with inorganic or organic acids, and agents, containing these compounds, for the oxidative dyeing of fibers.Type: GrantFiled: September 9, 2002Date of Patent: July 29, 2003Assignee: Wella AGInventors: Laurent Chassot, Hans-Juergen Braun
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Patent number: 6599918Abstract: This invention is directed to substituted (aminoiminomethyl or aminomethyl) dihydrobenzofurans and benzopyrans that inhibit Factor Xa, pharmaceutical compositions comprising these compounds and their use for inhibiting Factor Xa or treating pathological conditions in a patient that may be ameliorated by administration of such compounds. This invention is also is also directed to substituted (aminoiminomethyl or aminomethyl) dihydrobenzofurans and benzopyrans which directly inhibit both Factor Xa and Factor IIa (thrombin), to pharmaceutical compositions comprising these compounds, to intermediates useful for preparing these compounds and to a method of simultaneously directly inhibiting both Factor Xa and Factor IIa (thrombin).Type: GrantFiled: February 22, 2002Date of Patent: July 29, 2003Assignee: Aventis Pharmaceuticals Inc.Inventors: Christopher J. Burns, William P. Dankulich, Daniel G. McGarry, Francis A. Volz
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Patent number: 6593357Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formula: where R1-4, Q, and T are described in the specification. The compounds are useful for treating disease states in mammals that are alleviated by a protein kinase inhibitor, particularly diseases such as cancer, inflammatory disorders, restenosis, and cardiovascular disease.Type: GrantFiled: August 22, 2002Date of Patent: July 15, 2003Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jeremy Green, Jingrong Cao, Michael Hale, Christopher Baker, Francois Maltais, James Janetka, Michael Mullican, Guy Bemis, Xiaoling Xie, Judith Straub, Qing Tang
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Publication number: 20030109709Abstract: Provided are processes and chemical intermediates useful for preparing a compound of the formula I 1Type: ApplicationFiled: September 18, 2002Publication date: June 12, 2003Inventors: M.V. Ramana Reddy, Stanley C. Bell
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Patent number: 6573219Abstract: The invention relates to novel substituted heterocyclyl-2H-chromenes of the general formula (I) in which R1, R2, R3, R4, R5 Z are each as defined in the description, and to a process for their preparation and to their use as herbicides.Type: GrantFiled: February 5, 2002Date of Patent: June 3, 2003Assignee: Bayer AktiengesellschaftInventors: Karl-Heinz Linker, Roland Andree, Karl-Julius Reubke, Otto Schallner, Mark Wilhelm Drewes, Peter Dahmen, Dieter Feucht, Rolf Pontzen
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Patent number: 6569860Abstract: This invention relates to compounds which are IP receptor antagonists and which are represented by Formula (I): wherein G2 is a heteroaryl group containing one or two nitrogen atoms substituted with a carboxylic acid group, said heteroaryl ring containing one or two nitrogen atoms, and G1 is as defined in the specification; or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and methods of preparation thereof.Type: GrantFiled: March 1, 2002Date of Patent: May 27, 2003Assignee: Roćhe Palo Alto LLCInventors: Francisco Javier Lopez-Tapia, Dov Nitzan, Counde O'Yang
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Publication number: 20030092740Abstract: The present application describes inhibitors of factor Xa with a neutral P1 specificity group of formula I: 1Type: ApplicationFiled: May 16, 2002Publication date: May 15, 2003Inventors: Robert A. Galemmo, Celia Dominguez, John M. Fevig, Qi Han, Patrick Y. Lam, Donald J.P. Pinto, James R. Pruitt, Mimi L. Quan
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Publication number: 20030069258Abstract: The present application describes nitrogen containing heteroaromatics and derivatives thereof of formula I: 1Type: ApplicationFiled: March 13, 2002Publication date: April 10, 2003Inventors: Patrick Y. Lam, Charles G. Clark, Celia Dominguez, John M. Fevig, Amy Qi Han, Renhua Li, Donald J. Pinto, James R. Pruitt, Mimi L. Quan
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Publication number: 20030069241Abstract: This invention relates to 1-diphenylmethyl-pyrazole derivatives of formula (I): 1Type: ApplicationFiled: July 23, 2002Publication date: April 10, 2003Inventors: Stanton F. Mchardy, Michael G. Vetelino
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Patent number: 6545031Abstract: Novel pyrroles, pyrazoles and triazoles, pharmaceutical compositions containing these compounds and their use as endothelin receptor antagonists as described.Type: GrantFiled: October 30, 2000Date of Patent: April 8, 2003Assignee: SmithKline Beecham CorporationInventors: Juan Ignacio Luengo, John Duncan Elliott, Jia-Ning Xiang
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Patent number: 6541423Abstract: The invention relates to pyrazolyl derivatives of benzo-condensated, unsaturated 5-membered nitrogen heterocycles of the general formula (I), wherein X represents N or a group C—R3; Y is O, S, SO, SO2 or NR4 or X—Y is S═N, and wherein X means sulfur, and the variables R1, R2 and Pz have the meanings indicated in claim 1. The invention, further relates to a method of producing said compounds, to agents that contain them and to their use as herbicidal agents.Type: GrantFiled: November 1, 2001Date of Patent: April 1, 2003Assignee: BASF AktiengesellschaftInventors: Guido Mayer, Ernst Baumann, Wolfgang von Deyn, Steffen Kudis, Klaus Langemann, Ulf Misslitz, Ulf Neidlein, Matthias Witschel, Michael Rack, Thorsten Volk, Martina Otten, Karl-Otto Westphalen, Helmut Walter
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Patent number: 6528509Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formula: where R1-4, Q, and T are described in the specification. The compounds are useful for treating disease states in mammals that are alleviated by a protein kinase inhibitor, particularly diseases such as cancer, inflammatory disorders, restenosis, and cardiovascular disease.Type: GrantFiled: October 5, 2001Date of Patent: March 4, 2003Assignee: Vertex Pharmacuticals, IncorporatedInventors: Michael Hale, Xiaoling Xie, Jeremy Green, Jingrong Cao, Christopher Baker, Francois Maltais, James Janetka, Guy Bemis, Michael Mullican, Judith Straub, Qing Tang, Robert Mashal
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Publication number: 20030040623Abstract: The present invention relates to specific photochromic h-annellated benzo[f]chromene derivatives and their use in synthetic resins of all types, especially for ophthalmic applications. In particular, the present invention relates to photochromic compounds derived from benzo[f]chromenes, which in the open form have especially long-wave absorption maxima making it possible to obtain violet to blue tints when used in phototropic glasses.Type: ApplicationFiled: May 10, 2002Publication date: February 27, 2003Inventors: Claudia Mann, Manfred Melzig, Udo Weigand
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Patent number: 6525086Abstract: The present invention relates to compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, A, X, T, Q, Z, U, Y, Ar, p and n are as defined in the specification. These 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: March 14, 2001Date of Patent: February 25, 2003Assignee: Novo Nordisk A/SInventors: Lone Jeppesen, Paul Stanley Bury, Per Sauerberg
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Publication number: 20030018058Abstract: The present invention describes compounds of formula I 1Type: ApplicationFiled: August 15, 2002Publication date: January 23, 2003Inventors: Mark E. Salvati, S. David Kimball
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Patent number: 6465395Abstract: The present invention provides thiochroman- and dihydrobenzothiophene-substituted methylene compounds of formula I. Further provided are compositions and methods utilizing said formula I compounds for the control of undesirable plant species.Type: GrantFiled: February 28, 2001Date of Patent: October 15, 2002Assignees: BASF Aktiengesellschaft, Idemitsu Kosan Company, Ltd.Inventors: Stephen S. Szucs, Kun-Jian Gu
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Patent number: 6462069Abstract: Amino-pyrazole compounds that modulate and/or inhibit the activity of protein kinases. These compounds and pharmaceutical compositions containing them are capable of mediating and/or inhibiting the activity cyclin-dependent kinases, thereby modulating and/or inhibiting unwanted cell proliferation. The invention is also directed to the therapeutic or prophylactic use of pharmaceutical compositions containing such compounds, and to methods of treating cancer as well as other disease states associated with unwanted angiogenesis and/or cellular proliferation, such as diabetic retinopathy, neovascular glaucoma, rheumatoid arthritis, and psoriasis, by administering effective amounts of such compounds.Type: GrantFiled: April 17, 2001Date of Patent: October 8, 2002Assignee: Agouron Pharmaceuticals, Inc.Inventors: Siegfried Heinz Reich, Michael B. Wallace
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Patent number: 6455703Abstract: 1,3,6-Trihydro-6-Aza-3-Oxapentalen-2-One Derivatives which have the following formula: wherein R1, R2, R3, R4, R5, Y, X, m, and n are as defined in the specification.Type: GrantFiled: December 6, 2000Date of Patent: September 24, 2002Assignee: Cell Pathways, Inc.Inventors: Gerhard Sperl, Rifat Pamukcu
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Patent number: 6455561Abstract: The present invention pertains to compositions and methods for treating disease states which are capable of being modulated by inhibition of phosphodiesterase IV or Tumour Necrosis Factor, or that is a pathological condition associated with a function of phosphodiesterase IV, eosinophil accumulation or a function of the eosinophil, said method comprising administering to a person or animal in need of such treatment an effective amount of the compound of a formula wherein R1 is C1-3 alkyl optionally substituted with one or more fluorines; R2 is CH2OCH3 or 2 or 3-tetrahydrofuranyl; R3 is a pyrazole, imidazole or isoxazole group of partial formula (A), (B) or (C) R4 is C 1-3 alkyl; and R5 and R6, which may be the same or different, each represents C1-3 alkyl, halogen, CF3 or CN; or a pharmaceutically-acceptable salt thereofType: GrantFiled: October 12, 2001Date of Patent: September 24, 2002Assignee: Darwin Discovery, Ltd.Inventors: Hazel Joan Dyke, Christopher Lowe, John Gary Montana
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Patent number: 6440899Abstract: Cyclohexenonedioxothiochromanoyl derivatives of the formula I where X is oxygen, sulfur, S═O, S(═O)2, CR4R5, C═O or C═NR6, the other substituents are as defined in the specification, and and agriculturally useful salts thereof; processes for preparing the cyclohexenonedioxotheiochromanoyl derivatives; compositions comprising them, and the use of these derivatives or of compositions comprising them for controling undesirable piants.Type: GrantFiled: October 30, 2000Date of Patent: August 27, 2002Assignee: BASF AktiengesellschaftInventors: Matthias Witschel, Klaus Langemann, Wolfgang von Deyn, Ulf Misslitz, Ernst Baumann, Stefan Engel, Guido Mayer, Ulf Neidlein, Oliver Wagner, Roland Götz, Martina Otten, Karl-Otto Westphalen, Helmut Walter
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Publication number: 20020115568Abstract: Disclosed are novel pyrazole derivatives which are free of phytotoxicity to corn and can control a broad range of cropland weeds at a low dosage and herbicides containing them, and the present invention provides pyrazole derivatives of the general formula (I), or salts thereof, 1Type: ApplicationFiled: February 13, 2002Publication date: August 22, 2002Applicant: Idemitsu Kosan Co. Ltd.Inventors: Kazufumi Nakamura, Kazuyoshi Koike, Masashi Sakamoto, Ichiro Nasuno
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Patent number: 6417189Abstract: The present invention relates to N-substituted cyclic aza compounds, pharmaceutical compositions comprising such compounds, and methods of their use for effecting neuronal activities.Type: GrantFiled: April 17, 2000Date of Patent: July 9, 2002Assignee: GPI NIL Holdings, Inc.Inventors: Yong-Qian Wu, Wei Huang, Gregory S. Hamilton
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Patent number: 6413913Abstract: The present invention provides a compound of formula I: wherein X is O or S(O)n; n is zero, 1 or 2; and Y is CR7R8, CHOR9, C(OR9)2, C═NOR10 or C═NNR20R21. Compounds of formula I are useful as herbicidal agents, particularly as agents for the control of undesirable plant species in the presence of a cereal crop.Type: GrantFiled: October 20, 2000Date of Patent: July 2, 2002Assignees: BASF Corporation, Idemitsu Kosen Company, Ltd.Inventor: Stephen S. Szucs
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Patent number: 6391901Abstract: 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: GrantFiled: January 21, 2000Date of Patent: May 21, 2002Assignee: Eli Lilly and CompanyInventors: 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
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Publication number: 20020058678Abstract: Disclosed are novel aromatic heterocyclic compounds of the formula(I) wherein Ar1, Ar2, L, Q and X are described herein. The compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are processes of making such compounds.Type: ApplicationFiled: June 12, 2001Publication date: May 16, 2002Inventors: Pier F. Cirillo, Thomas A. Gilmore, Eugene R. Hickey, John R. Regan, Lin-Hua Zhang
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Patent number: 6376519Abstract: Compounds of the formula wherein: X is selected from the group consisting of trihalomethyl, C1-C6 alkyl, and a group of formula II: wherein: R3 and R4 are independently selected from the group consisting of hydrogen; halogen; hydroxyl; nitro; C1-C6 alkyl; C1-C6 alkoxy; carboxy; C1-C6 trihaloalkyl; and cyano; Z is selected from the group consisting of substituted and unsubstituted aryl; or a pharmaceutically acceptable salt thereof. The compounds are inhibitors of cyclooxygenase-2 activity. They are useful for treating cyclooxygenase-mediated disorders, including, for example, inflamation, neoplastic disorders and angiogenesis-mediated disorders.Type: GrantFiled: June 16, 2000Date of Patent: April 23, 2002Assignee: Temple University-of the Commonwealth of Higher EducationInventors: E. Premkumar Reddy, M. V. Ramana Reddy
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Patent number: 6376527Abstract: The present invention relates to certain pyrazole derivatives of Formula (I): that are p-38 MAP kinase inhibitors, pharmaceutical compositions containing them, methods for their use, and methods for preparing these compounds.Type: GrantFiled: May 5, 1999Date of Patent: April 23, 2002Assignee: Syntex (U.S.A.) LLCInventors: David Michael Goldstein, Sharada Shenvi Labadie, David Mark Rotstein, Eric Brian Sjogren, Francisco Xavier Talamas
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Publication number: 20020045654Abstract: This invention provides a compound of the formula: 1Type: ApplicationFiled: April 24, 2001Publication date: April 18, 2002Inventors: Kazuo Ando, Tomoki Kato, Akiyoshi Kawai, Tomomi Nonomura
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Patent number: 6369225Abstract: Compounds having Formula 8 wherein the symbols have the meaning defined in the specification are inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids.Type: GrantFiled: August 29, 2000Date of Patent: April 9, 2002Assignee: Allergan Sales, Inc.Inventors: Jayasree Vasudevan, Alan T. Johnson, Dehua Huang, Roshantha A. Chandraratna
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Publication number: 20020028936Abstract: 1,3-Disubstituted Indolin-2-Ones compounds are useful in the treatment of neoplasia.Type: ApplicationFiled: September 28, 2001Publication date: March 7, 2002Inventors: Gerhard Sperl, Xiaojing Wang, Gary A. Piazza, Rifat Pamukcu
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Publication number: 20020028841Abstract: The invention is directed to substituted thieno[2,3-b]pyrrolidin-5-ones. The compounds are useful as inhibitors of cellular production of tumor necrosis factor (TNF-&agr;) and as antiproliferative agents. These compounds are useful in the treatment or control of neuro-degenerative diseases, cardiovascular diseases, cancer or inflammatory diseases.Type: ApplicationFiled: June 26, 2001Publication date: March 7, 2002Inventors: Adrian Liam Gill, William Harris
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Patent number: 6353102Abstract: Described are novel photochromic naphtho[1,2-b]pyran compounds having certain substituents at the 2 position of the pyran ring, certain substituents at the 5 and 6 positions and optionally at the 7, 8, 9 and 10-positions of the naphtho portion of the compound. These compounds may be represented by the following graphic formula: Also described are polymeric organic host materials that contain or that are coated with such compounds. Optically clear articles such as ophthalmic lenses or contact lenses that incorporate the novel naphthopyran compounds or combinations thereof with complementary photochromic compounds, e.g., certain other naphthopyrans, benzopyrans, and spiro(indoline)type compounds, are also described.Type: GrantFiled: December 17, 1999Date of Patent: March 5, 2002Assignee: PPG Industries Ohio, Inc.Inventor: Anil Kumar
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Patent number: 6352959Abstract: Thiochromanoylpyrazolone derivatives of the formula I where: A is an unsubstituted or substituted, saturated or unsaturated alkyl chain; R1 is cyano, thiocyanato, nitro, OR4, SR5, SOR6, S02R6, ONR6NR7, ON═CR6R8, NR9R10, P(O)R11R12, P(S)R11R12, COR, CO2R6, unsubstituted or substituted phenyl or heterocyclyl; R2 is alkyl, haloalkyl, alkoxy or haloalkoxy; R3 is hydrogen, alkyl or halogen; X is oxygen, sulfur, S═O, S(═O)2, CR13R14, C═O or C═NR15; m is 0, 1 or 2; n is 0, 1, 2, 3 or 4; R16 is substituted pyrazol-4-yl-carbonyl or substituted (4,5-dihydro-5-oxo-pyrazol-4-yl)methylidene; and their agriculturally useful salts; Processes for preparing the thiochromanoylpyrazolone derivatives, compositions comprising them, and the use of these derivatives or of the compositions comprising them for controlling undesirable plants are described.Type: GrantFiled: May 31, 2001Date of Patent: March 5, 2002Assignee: BASF AktiengesellschaftInventors: Klaus Langemann, Ernst Baumann, Wolfgang von Deyn, Steffen Kudis, Guido Mayer, Ulf Misslitz, Ulf Neidlein, Matthias Witschel, Norbert Götz, Martina Otten, Karl-Otto Westphalen, Helmut Walter
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Publication number: 20020022645Abstract: The present invention pertains to compositions and methods for treating disease states which are capable of being modulated by inhibition of phosphodiesterase IV or Tumour Necrosis Factor, or that is a pathological condition associated with a function of phosphodiesterase IV, eosinophil accumulation or a function of the eosinophil, said method comprising administering to a person or animal in need of such treatment an effective amount of the compound of a formula 1Type: ApplicationFiled: October 12, 2001Publication date: February 21, 2002Inventors: Hazel Joan Dyke, Christopher Lowe, John Gary Montana
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Publication number: 20020016262Abstract: Disclosed are novel pyrazole derivatives which are free of phytotoxicity to corn and can control a broad range of cropland weeds at a low dosage and herbicides containing them, and the present invention provides pyrazole derivatives of the general formula (I), or salts thereof, 1Type: ApplicationFiled: July 23, 2001Publication date: February 7, 2002Applicant: IDEMITSU KOSAN CO., LTD.Inventors: Kazufumi Nakamura, Kazuyoshi Koike, Masashi Sakamoto, Ichiro Nasuno
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Patent number: 6340694Abstract: The diarylbenzopyran derivatives represented by formula I, and the pharmaceutically acceptable salts thereof, are disclosed. The composition comprising the compound of formula I, or a pharmaceutically acceptable salt thereof, shows an excellent selective inhibition of cyclooxygenase-2.Type: GrantFiled: February 20, 2001Date of Patent: January 22, 2002Assignee: Pacific CorporationInventors: Yung Hyup Joo, Chang Hoon Lee, Min-Soo Noh, Jun-Yong Ha, Jin Kyu Choi, Kyung Min Lim, Jin Kwan Kim, Seon-Hwa Kang
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Patent number: 6339099Abstract: The present application describes nitrogen containing heteroaromatics and derivatives thereof of formula I: or pharmaceutically acceptable salt forms thereof, wherein rings D—E represent guanidine mimics, which are useful as inhibitors of factor Xa.Type: GrantFiled: June 18, 1998Date of Patent: January 15, 2002Assignee: DuPont Pharmaceuticals CompanyInventors: Patrick Y. Lam, Charles G. Clark, Celia Dominguez, John M. Fevig, Qi Han, Renhua Li, Donald J. P. Pinto, James R. Pruitt, Mimi L. Quan
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Patent number: 6335345Abstract: Spiro compounds of the general formula (I): wherein Ar1 represents an optionally substituted aryl or heteroaryl; n represents 0 or 1; T, U, V and W each represent a nitrogen atom or an optionally substituted methine group, wherein at least two of which represent said methine group; X represents methine; Y represents an optionally substituted imino or oxygen atom. These novel spiro compounds exhibit neuropeptide Y receptor (NPY) antagonistic activities and are useful as agents for the treatment of various diseases related to NPY, for example, cardiovascular disorders, central nervous system disorders, metobolic diseases and the like.Type: GrantFiled: August 14, 2001Date of Patent: January 1, 2002Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Takehiro Fukami, Akio Kanatani, Akane Ishihara, Yasuyuki Ishii, Toshiyuki Takahashi, Yuji Haga, Toshihiro Sakamoto, Takahiro Itoh
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Patent number: 6335357Abstract: A 1-aryl-3-cyano-5-(het)arylalkylaminopyrazole derivative represented by the general formula (1): process of making, intermediate thereof and pesticide therewith.Type: GrantFiled: October 7, 1999Date of Patent: January 1, 2002Assignee: Mitsubishi Chemical CorporationInventors: Shuko Okui, Nobuo Kyomura, Toshiki Fukuchi, Ken Tanaka
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Publication number: 20010053788Abstract: The present invention relates, among many things, to novel 4,5-dihydro-1H-pyrazole compounds which can be potent antagonists of the cannabis CB1-receptor.Type: ApplicationFiled: March 23, 2001Publication date: December 20, 2001Applicant: Solvay Pharmaceuticals B.V.Inventors: Josephus H. M. Lange, Cornelis G. Kruse, Jacobus Tipker, Martinus T. M. Tulp, Bernard J. Van Vliet
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Patent number: 6331556Abstract: A compound of the formula wherein R1 is C1-3 alkyl optionally substituted with one or more fluorines; R2 is CH2OCH3 or 2 or 3-tetrahydrofuranyl; R3 is a pyrazole, imidazole or isoxazole group of partial formula (A), (B) or (C) R4 is C1-3 alkyl; and R5 and R6, which may be the same or different, each represents C1-3 alkyl, halogen, CF3 or CN; or a pharmaceutically-acceptable salt thereof.Type: GrantFiled: February 9, 2001Date of Patent: December 18, 2001Assignee: Darwin Discovery, Ltd.Inventors: Hazel Joan Dyke, Christopher Lowe, John Gary Montana
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Publication number: 20010051733Abstract: The present invention relates to pyrazole derivatives of the formula (I), 1Type: ApplicationFiled: February 13, 2001Publication date: December 13, 2001Applicant: IDEMITSU KOSAN COMPANY, LIMITEDInventors: Kazufumi Nakamura, Masashi Sakamoto, Ichiro Nasuno
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Patent number: 6326333Abstract: Pyrazolyldioxothiochromanoyl derivatives of the formula I where: X is oxygen, sulfur, S═O, S(═O)2, CR4R5, C═O or C═NR6, R1 is hydrogen, nitro, halogen, cyano, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio, haloalkylthio, alkylsulfinyl, haloalkylsulfinyl, alkylsulfonyl, haloalkylsulfonyl, aminosulfonyl with or without substitution or sulfonylamino with or without substitution; R2 is alkyl, haloalkyl, alkoxy or haloalkoxy; R3 is hydrogen, alkyl or halogen; R4, R5 are hydrogen, nitro, halogen, cyano, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio, haloalkylthio, alkylsulfinyl, haloalkylsulfinyl, alkylsulfonyl, haloalkylsulfonyl or substituted amino; or R4 and R5 together form a chain which may be substituted and/or interrupted by oxygen or sulfur; or a methylidene group with or without substitution; l is 0 to 4; R7 is substituted pyrazol-4-ylcarbonyl or substituted pyrazol-4-ylmethylidene; and agriculturally useful salts thereof.Type: GrantFiled: November 8, 2000Date of Patent: December 4, 2001Assignee: BASF AktiengesellschaftInventors: Matthias Witschel, Klaus Langemann, Wolfgang von Deyn, Ulf Misslitz, Ernst Baumann, Stefan Engel, Guido Mayer, Ulf Neidlein, Oliver Wagner, Martina Otten, Karl-Otto Westphalen, Helmut Walter
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Publication number: 20010031777Abstract: A compound of the formula 1Type: ApplicationFiled: February 9, 2001Publication date: October 18, 2001Inventors: Hazel Joan Dyke, Christopher Lowe, John Gary Montana