The Additional Hetero Ring Is A Diazine Patents (Class 514/252.02)
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Patent number: 6562817Abstract: The present invention provides a compound of the formula (I): wherein A ring, B ring and C ring are each independently optionally substituted aromatic carbocycle or optionally substituted 5- or 6-membered heterocycle which may fuse with benzene ring, W1, W2 and/or W3 represents a bond when A ring, B ring and/or C ring is optionally substituted 5-membered heterocycle, X is —O—, —NR1— wherein R1 is hydrogen, lower alkyl etc. or the like, Y is hydrogen, lower alkyl, lower alkenyl or the like, one of V1 and V2 is a bond, and the other is a bond, —O— or the like, and a pharmaceutical composition comprising the same.Type: GrantFiled: July 21, 2000Date of Patent: May 13, 2003Assignee: Shionogi & Co., Ltd.Inventors: Norihiko Tanimoto, Yasushi Hasegawa, Nobuhiro Haga
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Publication number: 20030087905Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases.Type: ApplicationFiled: May 23, 2002Publication date: May 8, 2003Applicant: G.D. Searle & Co.Inventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Publication number: 20030087906Abstract: The compounds of the present invention are 2,6,9-trisubstituted purine derivatives which are inhibitors of cyclin/cdk complexes. The compounds of the current invention also are potent inhibitors of human cellular proliferation. As such, the compounds of the present invention constitute pharmaceutical compositions with a pharmaceutically acceptable carrier. Such compounds are useful in treating a disorder mediated by elevated levels of cell proliferation in a mammal compared to a healthy mammal by administering to such mammal an effective amount of the compound.Type: ApplicationFiled: September 11, 2001Publication date: May 8, 2003Inventor: Michael Peter Trova
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Publication number: 20030083331Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases.Type: ApplicationFiled: May 23, 2002Publication date: May 1, 2003Applicant: G.D. Searle & Co.Inventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Publication number: 20030083327Abstract: This invention describes novel pyrazole compositions comprising a pharmaceutically acceptable carrier and a compound of formula VIII: 1Type: ApplicationFiled: September 14, 2001Publication date: May 1, 2003Inventors: Robert Davies, Pan Li
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Publication number: 20030083269Abstract: Disclosed are compounds that inhibit the microbial NAD synthetase enzyme. For example, disclosed are compounds of the formula Ar1—X—Ar2—Y—L—Z—Q, wherein Q is Q1Ar3 or Ar3Q1; Ar1, Ar2, and Ar3 are independently aryl or heteroaryl, optionally substituted with one or more substituents; X, Y, and Z are independently selected from the group consisting of a covalent bond or groups containing one or more of C, H, N, O, S atoms; L is a linker and Q1 is an alkylenyl, alkylenyl carbonyloxy alkyl, or alkylenyl carbonylamino alkyl group, optionally having a substituent; a covalent bond; a group containing amidine or guanidine function wherein the amidine or guanidine may be optionally N-substituted with an alkyl; or a zwitterion; or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: February 22, 2002Publication date: May 1, 2003Applicant: Virtual Drug Development, Inc.Inventors: Wayne J. Brouillette, Lawrence DeLucas, Christie Brouillette, Sadanandan E. Velu, Yong-Chul Kim, Liyuan Mou, R. Stephen Porter
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Patent number: 6555539Abstract: Indazole compounds that modulate and/or inhibit cell proliferation, such as the activity of protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating, e.g., kinases-dependent diseases to modulate and/or inhibit 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: January 18, 2001Date of Patent: April 29, 2003Assignee: Agouron PharmaceuticalsInventors: Siegfried Heinz Reich, Ted Michael Bleckman, Susan Elizabeth Kephart, William Henry Romines, Michael B. Wallace
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Publication number: 20030078264Abstract: The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(n+1)-Alkanol compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Novel high yield, stereoselective processes for the preparation of the chiral substituted alkanol compounds from chiral and achiral intermediates are described. Preferred (R)-Chiral 1-Substitutedamino-(n+1)-Alkanol compounds are substituted (R)-Chiral N,N-bis-benzyl aminoalcohols.Type: ApplicationFiled: December 12, 2001Publication date: April 24, 2003Inventors: James A. Sikorski, Richard C. Durley, Margaret L. Grapperhaus, Mark A. Massa, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Brian S. Hickory, Monica B. Norton, William F. Vernier, Deborah A. Mischke, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Publication number: 20030078236Abstract: According to the invention there is provided a compound the formula I; 1Type: ApplicationFiled: August 29, 2002Publication date: April 24, 2003Applicant: Allergan, Inc.Inventors: Robert M. Burk, Sophie Beauchemin
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Publication number: 20030073672Abstract: A method for treating an allergic condition, including an atopic allergic condition, using substituted pyrazoles.Type: ApplicationFiled: September 5, 2001Publication date: April 17, 2003Inventors: J. Guy Breitenbucher, Hui Cai, James P. Edwards, Cheryl A. Grice, Yin Gu, Darin J. Gustin, Lars Karlsson, Haripada Khatuya, Steven P. Meduna, Barbara A. Pio, Siquan Sun, Kevin L. Tays, Robin L. Thumond, Jianmei Wei
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Patent number: 6548512Abstract: The present application describes nitrogen containing heteroaromatics and derivatives thereof of formula I: or pharmaceutically acceptable salt or prodrug forms thereof, wherein J is N or NH and D may be C(═NH)NH2, which are useful as inhibitors of factor Xa.Type: GrantFiled: January 27, 2000Date of Patent: April 15, 2003Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Donald Joseph Phillip Pinto, James Russell Pruitt, Joseph Cacciola, John Matthew Fevig, Qi Han, Michael James Orwat, Mimi Lifen Quan, Karen Anita Rossi
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Publication number: 20030069240Abstract: A method for treating an allergic condition, including an atopic allergic condition, using substituted pyrazoles.Type: ApplicationFiled: February 13, 2002Publication date: April 10, 2003Inventors: J. Guy Breitenbucher, Hui Cai, James P. Edwards, Cheryl A. Grice, Yin Gu, Darin J. Gustin, Lars Karlsson, Haripada Khatuya, Steven P. Meduna, Barbara A. Pio, Siquan Sun, Kevin L. Tays, Robin L. Thurmond, Jianmei Wei
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Publication number: 20030069250Abstract: Novel benzamide 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: April 1, 2002Publication date: April 10, 2003Inventors: Bing-Yan Zhu, Penglie Zhang, Erick A. Goldman, Zhaozhong Jon Jia, Shawn Bauer, Wenrong Huang, John Woolfrey, Robert M. Scarborough
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Publication number: 20030064982Abstract: This invention describes novel protein kinase inhibitors of formula VII: 1Type: ApplicationFiled: September 14, 2001Publication date: April 3, 2003Inventors: Robert Davies, Pan Li
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Publication number: 20030064981Abstract: This invention describes novel pyrazole compositions comprising a pharmaceutically acceptable carrier and a compound of formula V: 1Type: ApplicationFiled: September 14, 2001Publication date: April 3, 2003Inventors: Ronald Knegtel, David Bebbington, Hayley Binch, Julian Golec, Sanjay Patel, Jean-Damien Charrier, David Kay, Robert Davies, Pan Li, Marion Wannamaker, Cornelia Forster, Albert Pierce
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Publication number: 20030060470Abstract: Ortho, ortho-substituted nitrogen-containing bisaryl compounds, processes for their preparation, their use as medicaments, and pharmaceutical preparations including their use as antiarrhythmic active compounds, for example, for the treatment and prophylaxis of atrial arrhythmias, e.g. atrial fibrillation (AF) or atrial flutters.Type: ApplicationFiled: December 5, 2001Publication date: March 27, 2003Inventors: Stefan Peukert, Joachim Brendel, Horst Hemmerle, Heinz-Werner Kleemann
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Publication number: 20030050317Abstract: The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(n+1)-Alkanol compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Novel high yield, stereoselective processes for the preparation of the chiral substituted alkanol compounds from chiral and achiral intermediates are described.Type: ApplicationFiled: December 12, 2001Publication date: March 13, 2003Inventors: James A. Sikorski, Richard C. Durley, Margaret L. Grapperhaus, Mark A. Massa, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Brian S. Hickory, Monica B. Norton, William F. Vernier, Deborah A. Mischke, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Patent number: 6521621Abstract: This invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereoisomeric forms thereof, wherein n is 0, 1 or 2; m is 1 or 2, provided that if m is 2, then n is 1; p is 1 or 2; ═Q is ═O or ═NR3; X is a covalent bond or a bivalent radical of formula —O—, —S—, —NR3—; R1 is Ar1, Ar1C1-6alkyl or di(Ar1)C1-6alkyl, wherein each C1-6alkyl group is optionally substituted with hydroxy, C1-4alkyloxy, oxo or a ketalized oxo substituent; R2 is Ar2, Ar2C1-6alkyl, Het1 or Het1C1-6alkyl; R3 is hydrogen or C1-6alkyl; L is hydrogen; Ar3; C1-6alkyl; C1-6alkyl substituted with 1 or 2 substituents selected from hydroxy, C1-6alkyloxy, Ar3, Ar3C1-6alkyloxy and Het2; C3-6alkenyl; Ar3C3-6alkenyl; di(Ar3)C3-6alkenyl or a radical of formula (a-1), (a-2), (a-3), (a-4) or (a-5); Ar1, Ar2 and Ar3 are each phenyl or substituted phenyl; Het1 and Het2 are each monocyclic or a bicyclic heterocycles; as substancType: GrantFiled: December 22, 2000Date of Patent: February 18, 2003Assignee: Janssen Pharmaceutica N.V.Inventors: Frans Eduard Janssens, François Maria Sommen, Dominique Louis Nestor Ghislaine Surleraux, Joseph Elisabeth Leenaerts, Yves Emiel Maria Van Roosbroeck
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Publication number: 20030032644Abstract: Substituted Polycyclic Aryl and Heteroaryl tetiary-leteroalkylamines Useful for Inhibiting Cholesteryl Ester Transfer Protein Activity Abstract The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases.Type: ApplicationFiled: February 7, 2002Publication date: February 13, 2003Applicant: G.D. Searle & Co.Inventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Patent number: 6518273Abstract: The present invention relates to compounds of the formula (I): wherein R1a, R1b, R2, R3, R4, R5, X and n are defined herein. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migraine, emesis and postherpetic neuralgia.Type: GrantFiled: September 4, 2001Date of Patent: February 11, 2003Assignee: Merck Sharp & Dohme Ltd.Inventors: Kevin Tyler Chapman, Kevin Dinnell, Jason Matthew Elliott, Gregory John Hollingworth, Steven Michael Hutchins, Duncan Edward Shaw, Christopher Alan Willoughby
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Patent number: 6518271Abstract: Corticotropin releasing factor (CRF) antagonists of formula I: and their use in treating anxiety, depression, and other psychiatric, neurological disorders as well as treatment of immunological, cardiovascular or heart-related diseases and colonic hypersensitivity associated with psychopathological disturbance and stress.Type: GrantFiled: August 9, 2000Date of Patent: February 11, 2003Assignee: Bristol-Myers Squibb CompanyInventors: Paul Joseph Gilligan, Rajagopal Bakthavatchalam
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Publication number: 20030027828Abstract: Compounds of formula I, 1Type: ApplicationFiled: October 1, 2001Publication date: February 6, 2003Inventors: Manfred Schudok, Otmar Klingler, Hans-Peter Nestler, Hans Matter, Herman Schreuder
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Patent number: 6514982Abstract: CRF receptor antagonists are disclosed which have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in a warm-blooded animals, such as stroke. The CRF receptor antagonists of this invention have the following structure: including stereoisomers and pharmaceutically acceptable salts thereof, wherein n, m, A, B, C, R, R1, R2 and Ar are as defined herein.Type: GrantFiled: November 12, 1999Date of Patent: February 4, 2003Assignee: Neurocrine Biosciences, Inc.Inventors: Mustapha Haddach, Brian P. Dyck, Charles Q. Huang, Jodie Nelson, Zhiqiang Guo, James R. McCarthy
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Publication number: 20030013719Abstract: Ortho, meta-substituted bisaryl compounds, processes for their preparation, their use as medicaments, and pharmaceutical preparations including their use as antiarrhythmic active compounds, for example, for the treatment and prophylaxis of atrial arrhythmias, e.g. atrial fibrillation (AF) or atrial flutters.Type: ApplicationFiled: November 29, 2001Publication date: January 16, 2003Inventors: Stefan Peukert, Joachim Brendel, Horst Hemmerle, Heinz-Werner Kleeman
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Publication number: 20030013718Abstract: The invention relates to the treatment of an inflammatory disease, especially an inflammatory rheumatoid or rheumatic disease, and/or pain with an inhibitor of the activity of VEGF receptor tyrosine kinase of the formula I, 1Type: ApplicationFiled: September 26, 2001Publication date: January 16, 2003Inventors: Guido Bold, Janet Dawson King, Jorg Frei, Richard Heng, Paul William Manley, Bernhard Wietfeld, Jeanette Marjorie Wood
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Patent number: 6506754Abstract: The present invention provides compounds which have a pyrazinone or pyridinone ring at P3 and which feature a six member heterocyclic ring having two ring nitrogen atoms and the remainder of the ring atoms carbon atoms at P1. These compounds have biological activity as active and potent inhibitors of thrombin. Their pharmaceutically acceptable salts, pharmaceutical compositions thereof and methods of using these compounds and pharmaceutical compositions comprising these compounds as therapeutic agents for treatment of disease states in mammals which are characterized by abnormal thrombosis are also described.Type: GrantFiled: April 14, 2000Date of Patent: January 14, 2003Assignee: Corvas International, Inc.Inventors: Daniel Vanna Siev, Gian Luca Araldi, Jonathan Zhanqi Ho, John Eugene Reiner, Joseph Edward Semple
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Patent number: 6498162Abstract: The invention relates to new arylglycinamide derivatives of general formula I and the pharmaceutically acceptable salts thereof, wherein R1 and R2 together with the N to which they are bound form a ring of the formula in which R3, R4, R5, Ar, R6, R7, R8, R9, R10, R11, r, s and t have the meanings given in the specification and the preparation and use thereof. The new compounds are valuable neurokinin (tachykinin) antagonists.Type: GrantFiled: November 1, 2000Date of Patent: December 24, 2002Assignee: Boehringer Ingelheim Pharma KGInventors: Franz Esser, Gerd Schnorrenberg, Kurt Schromm, Horst Dollinger, Birgit Jung, Georg Speck
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Publication number: 20020193375Abstract: The invention relates to heterocyclic derivatives, or pharmaceutically-acceptable salts thereof, which possess antithrombotic and anticoagulant properties and are accordingly useful in methods of treatment of humans or animals. The, invention also relates to processes for the preparation of the heterocyclic derivatives, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments for use in the production of an antithrombotic or anticoagulant effect, formula (I).Type: ApplicationFiled: June 27, 2002Publication date: December 19, 2002Applicant: ZENECA LIMITEDInventors: Peter Warner, Roger James, Thorsten Nowak
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Patent number: 6486160Abstract: Disclosed is a pharmaceutical composition for modulating immunity, which comprises a benzimidazole, represented by the following general formula (I), a 3H tautomer, an optically active enantiomer or a pharmaceutically acceptable acid-addition salt thereof wherein, R represents an alkyl group having 1 to 5 carbon atoms, a hydroxyphenyl group or a methoxyphenyl group.Type: GrantFiled: April 23, 2001Date of Patent: November 26, 2002Assignee: Toray Industries, Inc.Inventor: Akira Matsumori
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Patent number: 6479484Abstract: The invention is directed to substituted 2-aminoacetamides represented by formula (II): and to pharmaceutically acceptable salts and prodrugs thereof, wherein the substituents are defined herein. The invention is also directed to the use of substituted 2-aminoacetamides in methods for the treatment of neuronal damage following global and focal ischemia, and for the treatment, prevention or amelioration of pain, as anticonvulsants, as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.Type: GrantFiled: August 8, 2000Date of Patent: November 12, 2002Assignee: Euro-Celtique S.A.Inventors: Nancy C. Lan, Yan Wang, Sui Xiong Cai
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Publication number: 20020165232Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases.Type: ApplicationFiled: November 14, 2001Publication date: November 7, 2002Inventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Publication number: 20020165236Abstract: Treatment of Protozoan Infections with new diphenylurea derivatives.Type: ApplicationFiled: December 12, 2001Publication date: November 7, 2002Inventors: Andrea Aschenbrenner, Katharina Aulinger Fuchs, Matthias Dormeyer, Gabriel Garcia, Bernd Kramer, Stefano Pegoraro, Jurgen Kraus, Rolf Krauss, Hans Leban, Wael Saeb, Kristina Wolf
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Publication number: 20020165231Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases.Type: ApplicationFiled: November 14, 2001Publication date: November 7, 2002Inventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Patent number: 6476016Abstract: Cyclic oxyguanidine pyrazinone compounds are described, including compounds of the Formula I: wherein R3, R4, R5, W, and A are as set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof. The compounds of the 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. Compositions for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation are described.Type: GrantFiled: July 17, 2001Date of Patent: November 5, 2002Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Aihua Wang, Bruce Edward Tomczuk, Tianbao Lu, Richard M. Soll, John Curtis Spurlino, Roger Francis Bone
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Patent number: 6469003Abstract: A pyridazinone derivative represented by formula (I): a pharmaceutically acceptable salt thereof, or a derivative thereof, or a pharmaceutical composition comprising as an active ingredient the derivative or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier or diluent.Type: GrantFiled: February 14, 2001Date of Patent: October 22, 2002Assignee: Nihon Nohyaku Co., Ltd.Inventors: Makoto Gotoh, Koji Umimoto, Masanobu Onishi, Akiyuki Satoh, Yoshitami Oshita, Masashi Nagamine
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Publication number: 20020143017Abstract: The present invention relates to novel pyridazinone compounds, pharmaceutical compositions comprising those compounds and to methods of using such compounds and compositions to inhibit aldose reductase, lower sorbitol levels and, thus, lower fructose levels, and/or treat or prevent diabetic complications such as diabetic neuropathy, diabetic retinopathy, diabetic nephropathy, diabetic cardiomyopathy, diabetic microangiopathy and diabetic macroangiopathy in mammals. This invention also relates to methods of affording cardioprotection to subjects not suffering from diabetes. This invention also relates to pharmaceutical compositions and kits comprising a combination of an aldose reductase inhibitor (ARI) of this invention and a sorbitol dehydrogenase inhibitor and to methods of using such compositions or kits to treat or prevent the above diabetic complications in mammals.Type: ApplicationFiled: March 21, 2002Publication date: October 3, 2002Inventor: Banavara L. Mylari
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Publication number: 20020132812Abstract: Compounds of formula (I) which are optionally substituted 2-(&ohgr;,&ohgr;-diarylalkyl)-4,5-dihydro-1H-imidazoles and 2-(&ohgr;,&ohgr;-diarylalkyl)-1,4,5,6-tetrahydropyrimidines and salts thereof with inorganic and organic acids have interesting pharmacological properties. Thus, the compounds are useful in the treatment of type 2 diabetes.Type: ApplicationFiled: November 9, 2001Publication date: September 19, 2002Inventors: Henrik Sune Andersen, Palle Jakobsen, Peter Madsen
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Patent number: 6448244Abstract: The present invention concerns novel water-soluble azole compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and stereochemically isomeric forms thereof; as antifungals; their processes for preparation, composition containing them and their use as a medicine.Type: GrantFiled: November 9, 2000Date of Patent: September 10, 2002Assignee: Janssen Pharmaceutica N.V.Inventors: Lieven Meerpoel, Leo Jacobus Jozef Backx, Louis Jozef Elisabeth Van der Veken
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Patent number: 6448242Abstract: The invention relates to compounds represented by the following general formula (1): wherein A is an aromatic compound which may be substituted, or the like, B is a nitrogen atom or CH, X is a lower alkylene group which may be substituted, or the like, Y is a single bond or the like; Z is a divalent residue of benzene which may be substituted, or the like, and m and n are independently an integer of 1 to 4, and medicines comprising such a compound. These compounds have an excellent inhibitory effect on the production of an IgE antibody and are hence useful as antiallergic agents and the like.Type: GrantFiled: August 21, 2000Date of Patent: September 10, 2002Assignee: Kowa Co., Ltd.Inventors: Hiroyuki Ishiwata, Seiichi Sato, Mototsugu Kabeya, Soichi Oda, Yukio Hattori, Makoto Suda, Manabu Shibasaki, Hiroshi Nakao, Takao Nagoya
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Patent number: 6440970Abstract: The present invention relates to diazabicyclic compounds, and preferably N-aryl diazabicyclic compounds. Of particular interest are 2-pyridyl diazabicyclic compounds, such as (1S,4S)-2-(3-pyridyl)-2,5-diazabicyclo[2.2.1]heptane. Other exemplary compounds of the present invention include: (1S,4S)-2-(5-(4-methoxyphenoxy)-3-pyridyl)-2,5-diazabicyclo[2.2.1]heptane, (1S,4S)-2-(5-pyrimidinyl)-2,5-diazabicyclo[2.2.1]heptane and (1S,4S)-2-(6-chloro-3-pyridazinyl)-2,5-diazabicyclo[2.2.1]heptane. The present invention also relates to prodrug derivatives of the compounds of the present invention.Type: GrantFiled: May 25, 2000Date of Patent: August 27, 2002Assignee: Targacept, Inc.Inventors: Thomas Jeffrey Clark, Gary Maurice Dull, Dwo Lynm, Lan Miao, Craig Harrison Miller, Jeffrey Daniel Schmitt
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Patent number: 6440976Abstract: Compounds described by the chemical structural formula or a pharmaceutically acceptable salt thereof, are useful in the treatment of pain, migraine, depression, anxiety, schizophrenia, Parkinson's disease, stroke, and in the treatment of neuropathies including postherpetic neuralgia, central pain from spinal cord injury, and phantom limb pain.Type: GrantFiled: June 25, 2001Date of Patent: August 27, 2002Assignee: Merck & Co., Inc.Inventors: David A. Claremon, John A. McCauley, Nigel J. Liverton, Cory R. Theberge
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Patent number: 6432950Abstract: Benzothienopyrimidine derivatives for inducing or promoting apoptosis and for arresting uncontrolled neoplastic cell proliferation, and specifically for arresting and treating neoplasia, including precancerous and cancerous lesions.Type: GrantFiled: July 12, 2000Date of Patent: August 13, 2002Assignee: Cell PathwaysInventors: Rifat Pamukcu, Gary A. Piazza
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Publication number: 20020103198Abstract: This invention relates to novel acylamino cyclopropane derivatives, processes for their preparation, pharmaceutical compositions containing them and their use as modulators of dopamine D3 receptors and for the treatment of anxiety, psychosis, substance abuse, Parkinson's disease, sexual dysfunction, and other central nervous system disorders.Type: ApplicationFiled: October 9, 2001Publication date: August 1, 2002Inventors: Anton F.J Fliri, Anthony R. Reinhold
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Publication number: 20020103203Abstract: Amide compounds that modulate and/or inhibit the activity of certain protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating tyrosine kinase signal transduction in order to modulate and/or inhibit 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: ApplicationFiled: January 19, 2001Publication date: August 1, 2002Inventors: Steven Lee Bender, Dilip Bhumralkar, Michael Raymond Collins, Stephen James Cripps, Judith Gail Deal, Lei Jia, Mitchell David Nambu, Cynthia Louise Palmer, Zhengwei Peng, Michael David Varney
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Patent number: 6426346Abstract: The present application describes 6-membered aromatics of formula I: or pharmaceutically acceptable salt forms thereof, wherein D may be CH2NH2 or C(═NH)NH2, which are useful as inhibitors of factor Xa.Type: GrantFiled: February 15, 2000Date of Patent: July 30, 2002Assignee: Bristol - Myers Squibb Pharma CompanyInventors: James Russell Pruitt, Donald Joseph Phillip Pinto, Mimi Lifen Ouan, Ruth Richmond Wexler
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Patent number: 6423716Abstract: The present invention relates to nitrogen-containing heterocyclic compounds represented by formula (I): wherein W represents 1,4-piperazinediyl, etc.; U represents NR1R2 (wherein R1 represents a hydrogen atom, a substituted or unsubstituted alkyl group, etc.; and R2 represents a hydrogen atom, etc. ), OR4, or SR5; V represents an oxygen atom, a sulfur atom, N—R6, or CR7R8, at least one of X, Y and Z represents a nitrogen atom, and the others are the same or different, and each represents a nitrogen atom or C—RA; and D1, D2, D3 and D4 each independently represent C—RB, a nitrogen atom, an oxygen atom, a sulfur atom, etc., optional adjoining two among D1 to D4 are combined to represent a nitrogen atom, N—R2A, an oxygen atom, a sulfur atom, etc.Type: GrantFiled: September 29, 2000Date of Patent: July 23, 2002Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Kenji Matsuno, Yuji Nomoto, Michio Ichimura, Shin-ichi Ide, Shoji Oda
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Patent number: 6423718Abstract: The present invention relates to 4,4-disubstituted-3,4-dihydro-2(1H)-quinazolinones of formula I: or stereoisomeric forms, stereoisomeric 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: August 2, 2000Date of Patent: July 23, 2002Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Jeffrey W. Corbett, Soo S. Ko
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Publication number: 20020094978Abstract: This invention relates to novel isoxazolines and isoxazoles of formula (I): 1Type: ApplicationFiled: July 13, 2001Publication date: July 18, 2002Inventors: Joanne M. Smallheer, Shuaige Wang, Prabhakar Jadhav
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Publication number: 20020091261Abstract: The invention relates to compounds of formula I, 1Type: ApplicationFiled: May 17, 2001Publication date: July 11, 2002Inventors: Guido Bold, Jorg Frei, Peter Traxler, Karl-Heinz Altmann, Helmut Mett, David Raymond Stover, Jeanette Marjorie Wood
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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