Additional Hetero Ring Containing Patents (Class 540/524)
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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: 6545148Abstract: The present invention relates to an improved process for preparing certain substituted caprolactam compounds which comprises acylating an aminocaprolactam compound with a lactone compound in the presence of a weak base and a polar, organic solvent, and hydrolyzing the resultant diamide compound in a mixture of solvents to obtain the desired caprolactam compound.Type: GrantFiled: March 11, 2002Date of Patent: April 8, 2003Assignee: Novartis AGInventors: David Daqiang Xu, Wenming Liu
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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: 6541467Abstract: The present invention provides compounds having a lactam ring at P3 and at P1 have a six-membered heterocyclic ring having two ring nitrogen ring atoms and the remainder of the ring atoms carbon atoms. 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: April 1, 2003Assignee: Corvas International, Inc.Inventors: Jonathan Zhanqi Ho, Joseph Edward Semple
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Publication number: 20030055041Abstract: The present invention relates to certain substituted caprolactam carbonate and ether compounds, pharmaceutical compositions containing said compounds, the use of said compounds in treating tumors and to a process for making said compounds.Type: ApplicationFiled: May 17, 2002Publication date: March 20, 2003Inventors: Frederick Ray Kinder, Richard William Versace, Kenneth Walter Bair
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Patent number: 6534495Abstract: The invention relates to a compound having the formula (I): R1SO2—B—X—Z—C(O)—Y, B is a bond, an amino acid of the formula —NR—CH[(CH2)pC(O)OH]—C(O)— or an ester derivative thereof wherein p is 1, 2, or 3, Gly, D-1-Piq, D-3-Piq, D-1-Tiq, D-3-Tiq, D-Atc, Aic, or a L- or D-amino acid having a hydrophobic, basic or neutral side chain; X is an amino acid with a hydrophobic side chain, glutamine, serine, theronine, a cyclic amino acid optionally containing an additional heteroatom selected from N, O or S, and optionally substituted with (1-6C)alkyl, (1-6C)alkoxy, benzyloxy or oxo, or X is 2-amino-isobutyric acid, —NR2—CH2—C(O)— or the fragment (I) or (II), wherein n is 2, 3, or 4, W is CH or N and R3 is H, (1-6C)alkyl or phenyl which groups may optionally be substituted with hydroxy, (1-6C)alkoxy, COOH, COO(1-6C)alkyl, CONH2, or halogen; Z is lysine or 4-aminocyclohexylglycine.Type: GrantFiled: October 26, 1999Date of Patent: March 18, 2003Assignee: Akzo NebelInventor: Anton Egbert Peter Adang
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Patent number: 6511973Abstract: Compound of the formula are inhibitors of the enzyme Factor Xa. These compounds are useful as anticoagulants in the treatment of cardiovascular diseases associated with thromboses.Type: GrantFiled: July 27, 2001Date of Patent: January 28, 2003Assignee: Bristol-Myers Squibb Co.Inventors: Philip D. Stein, Yan Shi, Stephen P. O'Connor, Chi Li
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Patent number: 6500818Abstract: Compounds having the following formula wherein L, M, R2, R3, R4, R5, R6, R7, X1 and X2 are as defined in the specification, pharmaceutically-acceptable salt thereof, useful for treating depression, anxiety, asthma, rheumatoid arthritis, Alzheimer's disease, cancer, schizophrenia, oedema, allergic rhinitis, inflammation, pain, gastrointestinal-hypermotility, emesis, Huntington's disease, psychoses, hypertension, migraine, bladder hypermotility, or urticaria, compositions including such compounds and processes for making such compounds.Type: GrantFiled: March 30, 2001Date of Patent: December 31, 2002Assignee: Astrazeneca ABInventors: Peter Robert Bernstein, Robert Frank Dedinas, Cyrus John Ohnmacht, Keith Russell
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Patent number: 6495540Abstract: This invention relates to novel lactams having the Formula (I): to their pharmaceutical compositions and to their methods of use. 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. More particularly, the present invention relates to the treatment of neurological disorders related to &bgr;-amyloid production such as Alzheimer's disease and Down's Syndrome.Type: GrantFiled: March 27, 2001Date of Patent: December 17, 2002Assignee: Bristol - Myers Squibb Pharma CompanyInventor: Lorin A. Thompson
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Patent number: 6495699Abstract: The present invention is directed to compound of the formula I: wherein R1, R2, R3, R4, R5, X, Y, and are as defined herein. These compounds are useful for inhibiting the activity of a metalloproteinase by contacting the metalloproteinase with an effective amount of the inventive compounds.Type: GrantFiled: August 6, 2001Date of Patent: December 17, 2002Assignee: Agouron Pharmaceuticals Inc.Inventors: Steven L. Bender, Arlindo L. Castelhano, Wesley K. M. Chong, Melwyn A. Abreo, Roland J. Billedeau, Jian Jeffrey Chen, Judith G. Deal
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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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Publication number: 20020147188Abstract: The present invention provides 4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel intermediates of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease, comprising inhibiting said bone loss or excessive cartilage or matrix degradation by administering to a patient in need thereof a compound of the present invention.Type: ApplicationFiled: February 13, 2002Publication date: October 10, 2002Applicant: SmithKline Beecham CorporationInventors: Robert Wells Marquis, Yu Ru, Daniel Frank Veber, Maxwell David Cummings, Scott Kevin Thompson, Dennis Shinji Yamashita
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Diazapane derivatives useful as antagonists of neurokinin 1 receptor and methods for their formation
Patent number: 6452001Abstract: The invention relates to compounds of the formula wherein R1, R2 are independently from each other aryl or heteroaryl, wherein the heteroaryl group contains one or two heteroatoms, selected from N, O, or S, and wherein the aryl or heteroaryl groups are optionally substituted by 1 to 3 substituents, which are independently from each other halogen, CF3, lower alkoxy or lower alkyl; R3 is hydrogen, lower alkyl, —(CH2)nN(R)2, —(CH2)n-heteroaryl or is a —(CH2)n-non aromatic heterocycle, which heterocycles are optionally substituted by halogen, CF3, lower alkoxy or lower alkyl; R4 is ═O, ═N(CH2)nCH3 or ═N(CH2)nN(R)2; R3 and R4 may be together with the N and C atoms to which they are attached the group —CR5═N—N═; R5 is hydrogen, —(CH2)nN(R)2, —(CH2)n-heteroaryl or is a —(CH2)n-non aromatic heterocycle, which heterocycles are optionally substituted by halogen, CF3, lower alkoxy or lower alkyl; R is hydrogen or lower alkyl;Type: GrantFiled: May 14, 2001Date of Patent: September 17, 2002Assignee: Hoffmann-La Roche Inc.Inventors: Guido Galley, Annick Goergler, Thierry Godel, Reinhard Heck -
Publication number: 20020128474Abstract: The present invention relates to an improved process for preparing certain substituted caprolactam compounds which comprises acylating an aminocaprolactam compound with a lactone compound in the presence of a weak base and a polar, organic solvent, and hydrolyzing the resultant diamide compound in a mixture of solvents to obtain the desired caprolactam compound.Type: ApplicationFiled: March 11, 2002Publication date: September 12, 2002Inventors: David Daqiang Xu, Wenming Liu
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Patent number: 6436980Abstract: Compounds are described which have efflux pump inhibitor activity. Also described are methods of using such efflux pump inhibitor compounds and pharmaceutical compositions which include such compounds.Type: GrantFiled: November 28, 2000Date of Patent: August 20, 2002Assignee: Essential Therapeutics, Inc.Inventors: Roger Leger, Ving J. Lee, Miles She
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Patent number: 6426413Abstract: The present invention relates to novel classes of compounds which are caspase inhibitors, in particular interleukin-1&bgr; converting enzyme (“ICE”) inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting caspase activity and consequently, may be advantageously used as agents against interleukin-1-(“IL-1”), apoptosis-, interferon-&ggr; inducing factor-(IGIF), or interferon-&ggr;-(“IFN-&ggr;”) mediated diseases, including inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, and degenerative diseases.Type: GrantFiled: September 5, 2000Date of Patent: July 30, 2002Assignee: Vertex Pharmaceuticals IncorporatedInventors: Marion W. Wannamaker, Paul Charifson, David J. Lauffer, Michael D. Mullican
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Patent number: 6420415Abstract: Compounds represented by general formula (1) or salts thereof which have a matrix metalloprotease inhibitory activity and are useful as drugs, wherein the rings A and B represent each an optionally substituted homocycle or heterocycle, etc.; R1s are the same or different and each represents hydrogen, optionally substituted hydrocarbyl, acyl, etc.; X1 represents a bond, optionally substituted divalent aliphatic hydrocarbyl, etc.; X2 represents a bond, optionally substituted divalent aliphatic hydrocarbyl, —O—, etc.; Ys are the same or different represents hydrogen, optionally substituted hydrocarbyl, oxo, etc.; m is 0 or 1; n is an integer of 1 to 3; q1 is an integer of 1 to 2n+4; and q2 is an integer of 0 to 2n+3, provided that q1+q2 is 2n+4.Type: GrantFiled: March 20, 2001Date of Patent: July 16, 2002Assignee: Takeda Chemical Industries, Ltd.Inventors: Toshiro Yamashita, Hiroshi Nara, Masayuki Takizawa, Koji Yoshimura
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Patent number: 6413954Abstract: The present invention relates to certain substituted caprolactam carbonate and ether compounds, pharmaceutical compositions containing said compounds, the use of said compounds in treating tumors and to a process for making said compounds.Type: GrantFiled: May 8, 2001Date of Patent: July 2, 2002Assignee: Novartis AGInventors: Frederick Ray Kinder, Jr., Richard William Versace, Kenneth Walter Bair
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Publication number: 20020061874Abstract: This invention relates to novel lactams having the Formula (I): 1Type: ApplicationFiled: April 3, 2001Publication date: May 23, 2002Inventors: Michael G. Yang, Hong Liu
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Patent number: 6384035Abstract: This invention relates a to a series of heterocyclic substituted piperazines of Formula I pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention selectively inhibit binding to the &agr;-1a adrenergic receptor, a receptor which has been implicated in benign prostatic hyperplasia. As such the compounds are potentially useful in the treatment of this disease.Type: GrantFiled: October 9, 1998Date of Patent: May 7, 2002Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Richard H. Hutchings, Haripada Khatuya, Gee-Hong Kuo, Xiaobing Li, William V. Murray, Catherine Prouty, Frank Villani, Nelson C. F. Yim, Cynthia Maryanoff
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Patent number: 6376484Abstract: A tetrazole derivatives of formula (I) wherein R1 is H, alkyl, alkoxy, carbocyclic ring, hetero ring, alkyl or alkoxy substituted by carbocyclic ring or hetero ring, etc.; AA1 is bond or AA2 is bond or AA1 and AA2, together, may have the formula (a); Y is the formula (b) (in which Tet ring is tetrazole; Z is alkylene, alkenylene, O, S, SO, SO2, NR26, methylene in alkylene replaced by O, S, —SO—, —SO2— or —NR26—; E is H, alkyl, COOR27 or in which Cyc is carbocyclic ring or hetero ring); a non-toxic salt thereof, an acid addition salt thereof or a hydrate thereof which has a pharmaceutical agents as an active ingredient. The compound of the formula (I) has an inhibitory effect on interleukin-1&bgr; converting enzyme, therefore, they are useful for prevention and/or treatment of various kinds of inflammatory disease.Type: GrantFiled: May 16, 2000Date of Patent: April 23, 2002Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Kazuyuki Ohmoto, Makoto Tanaka, Tohru Miyazaki, Hiroyuki Ohno
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Patent number: 6376485Abstract: Compounds of formula I in which R1, R2, R3 and A have the meaning set forth in the specification, are selective cyclic nucleotide phosphodiesterase (PDE) inhibitors useful as therapeutics in human and veterinary medicine. They are distinguished by low toxicity, good enteral absorption (high bioavailability), a wide therapeutic breadth and absence of significant side effects.Type: GrantFiled: January 3, 2001Date of Patent: April 23, 2002Assignee: Byk Gulden Lomberg Chemische Fabrik GmbHInventor: Thomas Martin
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Publication number: 20020045616Abstract: Compound of the formula 1Type: ApplicationFiled: July 27, 2001Publication date: April 18, 2002Inventors: Philip D. Stein, Yan Shi, Stephen P. O'Connor, Chi Li
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Publication number: 20020025957Abstract: Lactam inhibitors are provided which have the structure 1Type: ApplicationFiled: June 5, 2001Publication date: February 28, 2002Inventors: Philip D. Stein, Stephen P. O'Connor, Yan Shi, Chi Li
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Publication number: 20020025955Abstract: This invention relates to novel lactams of Formula (I): 1Type: ApplicationFiled: April 11, 2001Publication date: February 28, 2002Inventors: Qi Han, Hong Liu, Richard E. Olson, Michael G. Yang
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Patent number: 6344450Abstract: Lactam inhibitors are provided which have the structure X is wherein Y is O or S and R4 is R7O— or R8 and R1, R2, R3, R5, R6, R7, and R8, are as defined herein. These compounds are inhibitors of Factor Xa and thus are useful as anticoagulants, and are inhibitors of tryptase and thus are useful in treating asthma. Methods for treating cardiovascular diseases associated with thromboses and for treating asthma and related diseases are also provided.Type: GrantFiled: August 7, 2000Date of Patent: February 5, 2002Assignee: Bristol-Myers Squibb CompanyInventors: Gregory S. Bisacchi, Steven M. Seiler, R. Michael Lawrence, James C. Sutton, Jr., William A. Slusarchyk, Guohua Zhao
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Patent number: 6335443Abstract: A process for the synthetic generation of high affinity, iron binding compounds known as Exochelins, and more particularly, to a synthetic process for making Exochelins and to modifications to these newly synthesized compounds to vary their physiological properties, including applications of these newly synthesized and utile compounds for diagnosing and treating disease in mammals.Type: GrantFiled: March 5, 1999Date of Patent: January 1, 2002Assignee: Keystone Biomedical, Inc.Inventors: Leo S. Geraci, Stuart G. Levy, James P. Hudspeth, Richard L. Buswell, Jay F. Stearns
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Patent number: 6335326Abstract: The present invention relates to a group of novel benzisoxazole derivatives which are potent and selective antagonists of the dopamine D4-receptor.Type: GrantFiled: October 23, 2000Date of Patent: January 1, 2002Assignee: Duphar International Research B.V.Inventors: Jacobus A. J. Den Hartog, Gerben M. Visser, Bartholomeus J. Van Steen, Martinus T. M. Tulp, Eric Ronken, Cornelis G. Kruse, Josephus H. M. Lange
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Publication number: 20010044433Abstract: The present invention relates to certain substituted caprolactam compounds, pharmaceutical compositions containing said compounds, the use of said compounds in treating tumors and to a process for making said compounds.Type: ApplicationFiled: March 12, 2001Publication date: November 22, 2001Inventors: Frederick Ray Kinder, Kenneth Walter Bair, Christopher Turchik Jagoe, Richard William Versace, Sompong Wattanasin
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Patent number: 6319917Abstract: Compounds of formula I wherein R1, R1-R3, R4′, R4″ and R5 are as defined in the description, have valuable pharmaceutical properties and are effective especially as NK1 and NK2 antagonists. They are prepared in a manner known per se.Type: GrantFiled: September 5, 2000Date of Patent: November 20, 2001Assignee: Novartis AGInventors: Marc Gerspacher, Andreas von Sprecher, Robert Mah, Silvio Roggo, Stefan Stutz
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Patent number: 6316438Abstract: Compounds of the formula are useful as inhibitors of cGMP PDE especially Type 5.Type: GrantFiled: March 15, 2000Date of Patent: November 13, 2001Assignee: Bristol-Myers Squibb Co.Inventors: Guixue Yu, John Macor, Soojin Kim, Hyei-Jha Chung, Michael Humora, Kishta Katipally, Yizhe Wang
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Patent number: 6310058Abstract: Compounds represented by the formula [1] R1 is H or a substituent; R2 and R3 are C1-C3 alkyl; R4 is siderophore group e.g. CH3—(CH2)n—C(O)—N(OH)—(CH2)m— with n=10-22, m=2-6; X is O, S, or NH; X1 is O or NH; Y is H or alkyl; Z is H or substituted amino, e.g., t-BocNH or CbzNH, and r is 2-4; are useful in the method provided for treating tuberculosis. [1] is prepared by coupling [7], wherein HX1 is HO— or H2N—, with [4] obtained as the free acid after saponification of the methyl ester.Type: GrantFiled: May 25, 2000Date of Patent: October 30, 2001Assignee: University of Notre Dame du LacInventors: Marvin J. Miller, Yanping Xu
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Patent number: 6310057Abstract: This invention relates to &agr;-ketoamide inhibitors of multicatalytic protease (MCP), to compositions including such inhibitors, and to methods for the use of MCP inhibitors. The MCP inhibitors of the present invention are useful, for example, to retard loss of muscle mass incident to various physiological states.Type: GrantFiled: March 7, 2000Date of Patent: October 30, 2001Assignee: Cephalon, Inc.Inventors: Sankar Chatterjee, John P. Mallamo
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Patent number: 6303594Abstract: This invention relates to a series of arylsubstituted piperazines, of Formula I pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention selectively inhibit binding to the &agr;-1a adrenergic receptor, a receptor which has been implicated in benign prostatic hyperplasia. As such the compounds are potentially useful in the treatment of this and other disease.Type: GrantFiled: March 15, 2000Date of Patent: October 16, 2001Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Linda Jolliffe, William Murray, Virginia Pulito, Allan Reitz, Xiaobing Li, Linda Mulcahy, Cynthia Maryanoff, Frank Villani
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Patent number: 6303620Abstract: Disclosed are 4,4-disubstituted and 3,3-disubstituted piperidine compounds of formula I wherein D, E, G, J, R1, a, b, c, and d are defined in the specification, compositions containing them, and their use for treating medical disorders resulting from a deficiency in growth hormone.Type: GrantFiled: May 6, 1999Date of Patent: October 16, 2001Assignee: Novo Nordisk A/SInventors: Thomas Kruse Hansen, Michael Ankersen
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Patent number: 6297233Abstract: Caprolactam inhibitors are provided which have the structure including pharmaceutically acceptable salts thereof and all stereoisomers thereof, and prodrugs thereof, wherein n is 1 to 5; and and Y R1, R2, R3, R5, R5a, R6, R7, R8, R9 and R10 are as defined herein. These compounds are inhibitors of Factor Xa and thus are useful as anticoagulants. A method for treating cardiovascular diseases associated with thromboses is also provided.Type: GrantFiled: February 2, 2000Date of Patent: October 2, 2001Assignee: Bristol-Myers Squibb CompanyInventors: Philip D. Stein, Gregory S. Bisacchi, Yan Shi, Stephen P. O'Connor, Chi Li
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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: 6294549Abstract: A method for eliciting an &agr;v&bgr;5 or dual &agr;v&bgr;3/&agr;v&bgr;5 antagonizing effect in a mammal which comprises administering to the mammal a therapeutically effective amount of a compound of the formula which are useful for inhibiting restenosis, angiogenesis, atherosclerosis, diabetic retinopathy, macular degeneration, inflammation or tumor growth.Type: GrantFiled: July 23, 1998Date of Patent: September 25, 2001Assignee: Merck & Co., Inc.Inventors: George D. Hartman, Mark E. Duggan
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Patent number: 6284755Abstract: The present invention is directed to azepan-2-one compounds which inhibit prenyl-protein transferase, particularly farnesyl-protein transferase (Ftase), and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.Type: GrantFiled: December 7, 1999Date of Patent: September 4, 2001Assignee: Merck & Co., Inc.Inventors: S. Jane deSolms, Samuel L. Graham, Anthony W. Shaw, Terrence M. Ciccarone, Gerald E. Stokker
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Patent number: 6242438Abstract: The present invention provides compounds of formula (I) and the pharmaceutically acceptable salts thereof. Such compounds and salts are tachykinin antagonists.Type: GrantFiled: June 1, 1998Date of Patent: June 5, 2001Assignee: Pfizer Inc.Inventors: Alexander Roderick MacKenzie, Allan Patrick Marchington, Donald Stuart Middleton, Sandra Dora Meadows
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Patent number: 6239127Abstract: The present invention relates to certain substituted caprolactam compounds of formula (I), where R1 is (C1-6)alkyl or (C3-6)cycloalkyl; R2 hydrogen or (C1-6)alkyl; X is (C1-12)alkynylene; (C2-12)alkynylene; m is 0 or 1; and R3 is (C3-8)cycloalkyl; or an aromatic ring system selected from (II, III, IV and V), where R4 is hydrogen, chloro, or methoxy; R5 is hydrogen, chloro, (C1-18)alkyl or (C1-18)alkoxy, and Z is oxygen, sulfur, N—H, or N—CH3; or a pharmaceutically acceptable acid addition salt thereof, where possible, pharmaceutical compositions containing said compounds, the use of said compounds in treating tumors and to a process for making said compounds.Type: GrantFiled: November 17, 1999Date of Patent: May 29, 2001Assignee: Novartis AGInventors: Frederick Ray Kinder, Jr., Kenneth Walter Bair, Christopher Turchik Jagoe, Richard William Versace, Sompong Wattanasin
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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: 6194435Abstract: Novel lactams, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds of Formula I below: are useful in vitro or in vivo for preventing or treating coagulation disorders.Type: GrantFiled: October 10, 1997Date of Patent: February 27, 2001Assignee: Cor Therapeutics, Inc.Inventors: Bing-Yan Zhu, Robert M. Scarborough
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Patent number: 6174879Abstract: Aminocyclohexylester compounds, including thioesters, are disclosed. The compounds of the present invention may be incorporated in compositions and kits. The present invention also discloses a variety of in vitro and in vivo uses for the compounds and compositions, including the blockade of ion channels and the treatment of arrhythmias.Type: GrantFiled: March 17, 1999Date of Patent: January 16, 2001Assignee: University of British ColumbiaInventors: Bernard A. MacLeod, Michael J. A. Walker, Richard A. Wall
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Patent number: 6166040Abstract: Pharmaceutical compounds of the formula: ##STR1## in which n is 1 to 6, m is 1 or 2 and p is 1 or 2, R.sup.1 and R.sup.2 are each hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, HO--C.sub.1-4 alkyl, C.sub.1-4 alkoxy-C.sub.1-4 alkyl, C.sub.1-4 alkylthio, halo, optionally substituted phenyl, optionally substituted phenyl-C.sub.1-4 alkyl, or R.sup.1 and R.sup.2 together with the carbon atom to which they are attached form a C.sub.3-6 cycloalkyl group, >C.dbd.O, C.dbd.NOR' where R' is hydrogen or C.sub.1-4 alkyl,R.sup.3, R.sup.4 and R.sup.5 are each hydrogen, halo, nitro, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkyl-CO--, where m is 0, 1 or 2, R'R"N--SO.sub.2 --, --COOR', --CONR'R", --NR'R", --N(OR')COOR", --COR', --NHSO.sub.2 R', where R' and R' are each hydrogen or C.sub.1-4 alkyl,R.sup.6 and R.sup.7 are each hydrogen or C.sub.1-4 alkyl,X is oxygen or sulphur,the dotted line represents an optional double bond, and the fluorine atom is attached at the 6- or 7-position; and salts thereof.Type: GrantFiled: May 11, 1999Date of Patent: December 26, 2000Assignee: Eli Lilly and Company LimitedInventors: John Fairhurst, Peter Thaddeus Gallagher, Martin Victor Miles, William Martin Owton, Colin William Smith
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Patent number: 6124332Abstract: Therapeutically active hydroxamic acid derivatives, processes for their preparation, pharmaceutical compositions containing them, and the use of such compounds in medicine. The compounds are inhibitors of metalloproteinases involved in tissue degradation.Type: GrantFiled: February 3, 1999Date of Patent: September 26, 2000Assignee: British Biotech Pharmaceuticals Ltd.Inventors: Andrew Miller, Mark Whittaker, Raymond Paul Beckett
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Patent number: 6124333Abstract: Therapeutically active hydroxamic acid derivatives, processes for their preparation, pharmaceutical compositions containing them, and the use of such compounds in medicine. The compounds are inhibitors of metalloproteinases involved in tissue degradation.Type: GrantFiled: February 3, 1999Date of Patent: September 26, 2000Assignee: British Biotech Pharmaceuticals LimitedInventors: Andrew Miller, Mark Whittaker, Raymond Paul Beckett
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Patent number: 6124316Abstract: A compound of formula: ##STR1## in which: Ar represents a pyrid-2-yl or a phenyl which is unsubstituted or substituted by a halogen, a methyl or a (C.sub.1 -C.sub.4)alkoxy;R.sub.1 represents a methyl group;R.sub.11 represents hydrogen;or R.sub.1 and R.sub.11 together represent a --(CH.sub.2).sub.3 -- group;R.sub.2 represents a hydroxyl; a (C.sub.1 -C.sub.7)alkoxy; a (C.sub.1 -C.sub.7)acyloxy; a cyano; an --NR.sub.6 R.sub.7 group; an --NR.sub.3 COR.sub.4 group; an --NR.sub.3 COOR.sub.8 group; an --NR.sub.3 SO.sub.2 R.sub.9 group; an --NR.sub.3 CONR.sub.10 R.sub.12 group; a (C.sub.1 -C.sub.7)acyl group; a (C.sub.1 -C.sub.7)alkoxycarbonyl; a --CONR.sub.10 R.sub.12 group; a --CH.sub.2 OH group; a (C.sub.1 -C.sub.7)alkoxymethyl; a (C.sub.1 -C.sub.7)acyloxymethyl; a (C.sub.1 -C.sub.7)alkylaminocarbonyloxymethyl; a --CH.sub.2 NR.sub.13 R.sub.14 group; a --CH.sub.2 NR.sub.3 COR.sub.4 group; a --CH.sub.2 NR.sub.3 COOR.sub.8 group; a --CH.sub.2 NR.sub.3 SO.sub.2 R.sub.9 group; a --CH.sub.2 NR.sub.3 CONR.sub.10 R.sub.Type: GrantFiled: May 7, 1999Date of Patent: September 26, 2000Assignee: SanofiInventors: Daniel Bichon, Patrick Gueule, Didier Van Broeck, Xavier Emonds-Alt, Vincenzo Proietto
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Patent number: 6117870Abstract: A cyclic amide derivative of formula (I): ##STR1## wherein R.sup.1 represents a substituted alkyl group, a substituted alkenyl group, a substituted amino group, a substituted alkoxyl group, a substituted alkylthio group, a substituted carbamoyl group, a substituted sulfonamide group or a substituted amide group; the ring A represents a saturated cyclic alkyl group with 5 to 7 carbon atoms or a hetero-atom-containing saturated heterocyclic group with 3 to 6 carbon atoms; R.sup.2 represents a hydrogen atom, a substituted or unsubstituted alkyl group, a substituted or unsubstituted aromatic hydrocarbon group or a substituted or unsubstituted heterocyclic group; R.sup.3 represents a hydrogen atom, a group represented by the general formula R.sup.4 O-- or a group represented by the general formula R.sup.5 (R.sup.6)N-- wherein R.sup.Type: GrantFiled: November 10, 1999Date of Patent: September 12, 2000Assignee: Fujirebio Kabushiki KaishaInventors: Akihiko Hosoda, Nobuo Kobayashi, Naoko Tanabe, Tsuneo Koji, Masahiro Shibata, Akihiro Sekine, Masaharu Dozen