Acyclic Nitrogen Bonded Directly To A -c(=x)- Group, Wherein X Is Chalcogen Patents (Class 546/233)
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Patent number: 6509356Abstract: A class of substituted benzylnaphthylene compounds of the structure where R1 and R2 are independently hydrogen, alkyl of one to six carbon atoms, acyl of two to six carbon atoms, or phenacyl; X is —(CH2)1-6; Y is absent or is selected from 1,4-piperazinylene; ureido; N-(lower alkyl)ureido; N′-(lower alkyl)ureido; or N, N′-(di-lower alkyl ureido; and Z is 1-, 2- or 3-pyrrolidinyl; 1-, 2-, or 3-[1-(lower alkyl) pyrrolidinyl]; 1- 2-, 3- or 4-piperidinyl; 1-, 2-, 3- or 4-[1-lower alkyl)piperidinyl]; N,N-dialkyl; 1-azepinyl; 1- or 2-naphthylamino, 4-morpholinyl, dimethyl-4-morpholinyl, 3-azaspiro[5.Type: GrantFiled: August 4, 1998Date of Patent: January 21, 2003Assignee: Eli Lilly and CompanyInventors: Jeffrey Alan Dodge, Andrew Lawrence Glasebrook, Charles Willis Lugar, III
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Patent number: 6500823Abstract: The object of the invention consists of novel unsaturated hydroximic acid derivatives, the process for their preparation and as active substance such as compounds containing pharmaceutical compositions. The novel compounds possess valuable pharmaceutical effects, so they can be used in the treatment of states connected with energy deficiency of the cell caused by PARP inhibition, in diabetes complications, in oxygen deficient status of the heart and brain, in neurodegenerative diseases, in the treatment of autoimmune and/or viral diseases. In formula (I).Type: GrantFiled: March 2, 2001Date of Patent: December 31, 2002Assignee: N-Gene Research Laboratories, Inc.Inventors: Péter Literáti Nagy, Kálmán Takács, Balázs Sümegi
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Publication number: 20020193602Abstract: The present application relates to novel opioid receptor antagonists and agonists, methods of making these compounds, and methods of use thereof.Type: ApplicationFiled: March 19, 2002Publication date: December 19, 2002Applicant: Research Triangle InstituteInventors: Frank I. Carroll, James B. Thomas, S. Wayne Mascarella
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Publication number: 20020193634Abstract: Novel disulfide derivatives useful for preventing or treating allergic diseases of the eye, nose, skin, ear, gastrointestinal tract, airways or lung and preventing or treating manifestations of systemic mastocytosis are disclosed. The disulfide derivatives act as mast cell stabilizers.Type: ApplicationFiled: May 22, 2002Publication date: December 19, 2002Inventors: Zixia Feng, Mark R. Hellberg, Steven T. Miller
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Publication number: 20020169324Abstract: The present application relates to novel opioid receptor antagonists and agonists, methods of making these compounds, and methods of use thereof.Type: ApplicationFiled: March 19, 2002Publication date: November 14, 2002Applicant: Research Triangle InstituteInventors: Frank I. Carroll, James B. Thomas, S. Wayne Mascarella
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Patent number: 6479502Abstract: Compounds of formula (I) are matrix metalloprotemase inhibitors wherein X represents a carboxylic acid group —COOH, or a hydroxamic acid group —CONHOH;R2 represents a radical of formula (II): R3—(ALK)m—(Q)p—(ALK)n.Type: GrantFiled: February 21, 2001Date of Patent: November 12, 2002Assignee: British Biotech PharmaceuticalsInventor: Fionna Mitchell Martin
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Publication number: 20020165396Abstract: The present application relates to novel opioid receptor antagonists and agonists, methods of making these compounds, and methods of use thereof.Type: ApplicationFiled: March 19, 2002Publication date: November 7, 2002Applicant: Research Triangle InstituteInventors: Frank I. Carroll, James B. Thomas, S. Wayne Mascarella
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Patent number: 6476027Abstract: An N-hydroxy sulfonyl butanamide compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated N-hydroxy sulfonyl butanamide compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.Type: GrantFiled: December 6, 1999Date of Patent: November 5, 2002Assignee: Monsanto CompanyInventors: Clara I. Villamil, John N. Freskos, Brent V. Mischke, Patrick B. Mullins, Robert M. Heintz, Daniel P. Getman, Joseph J. McDonald, Gary A. DeCrescenzo, Thomas E. Barta, Daniel P. Becker
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Patent number: 6472394Abstract: Disclosed are compounds represented by structural formula I: or a pharmaceutically acceptable salt, ester or solvate thereof, wherein W is R1—CR3R12NR4C(O)— or R11C(O)NR4—; the dotted line is an optional double bond; X is —CHR8—, —C(O)—, or —C(═NOR9)—; Y is R1 is optionally substituted cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, heterocycloalkyl or heterocycloalkyl-alkyl; R2 is optionally substituted aryl or heteroaryl; R3 is alkyl, aryl or heteroaryl; R4 and R12 are H or alkyl; R8 is H, alkyl or alkoxyalkyl; R9 is H, alkyl or arylalkyl; R10 is H, alkyl or aryl; R11 is or, when R2 is R6-heteroaryl or R10 is not H, R11 can also be R5-phenylalkyl; n is 1-3 and m is 1-5; and R14 is 1-3 substituents selected from H, alkyl, halogen, —OH, alkoxy and CF3; and pharmaceutical compositions containing the compounds and methods of using the compounds in the trType: GrantFiled: December 17, 2001Date of Patent: October 29, 2002Assignee: Schering CorporationInventors: Brian A. McKittrick, Jing Su, John W. Clader, Shengjian Li, Guihau Guo
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Publication number: 20020151534Abstract: Antithrombotic compounds of general formula 1Type: ApplicationFiled: January 16, 2002Publication date: October 17, 2002Inventors: Uwe Joerg Ries, Henning Priepke, Herbert Nar, Jean-Marie Stassen, Wolfgang Wienen
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Patent number: 6465468Abstract: The subject invention concerns methods and compounds that have utility in the treatment of a condition associated with matrix metalloproteinase, ADAM or ADAM-TS enzymes, a condition that is mediated by TNF &agr; or a condition involving a membrane-shedding event that is mediated by a metalloproteinase. Compounds of the invention are of formula I (B)2N—X—(CH2)m—W—(CR1R2)n—COY (I) wherein n=0 or 1; m=0 or 1; X is S(O)1-2; Y is OH or NHOH; W is aryl or heteroaryl; and the other groups are as defined herein.Type: GrantFiled: March 22, 2000Date of Patent: October 15, 2002Assignee: Darwin Discovery LimitedInventors: Andrew Douglas Baxter, David Alan Owen, Duncan Batty, Robert John Watson
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Patent number: 6458957Abstract: This disclosure relates to the use of &agr;,&agr;-dibromo-&agr;-chloroacetophenone compounds as intermediates for the preparation of aromatic carbonyl compounds, especially aromatic amides. The compound 2,5-bis(2,2,2-trifluoroethoxy)-&agr;,&agr;-dibromo-&agr;-chloroacetophenone is especially useful as an intermediate for the preparation of flecainide, a known pharmaceutical.Type: GrantFiled: July 12, 2000Date of Patent: October 1, 2002Assignee: Geneva Pharmaceuticals, Inc.Inventors: Anup K. Ray, Hiren Patel, Shilpa V. Merai, Mahendra R. Patel
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Patent number: 6455549Abstract: A pharmaceutical composition, especially a pharmaceutical composition for the alleviation or treatment of symptoms due to ischemic diseases and symptoms derived from seizures, epilepsy, and migraine, and a Ca2+ overload suppressant, containing an arylpiperidinol or arylpiperidine derivative having the formula (I): wherein, R is H, an optionally substituted phenyl, an optionally substituted phenoxy, or an optionally substituted benzoyl, A is a connecting bond, a cycloalkylene, or an alkenylene optionally substituted with a lower alkyl, B is an alkylene optionally substituted with OH or an alkoxy or —NHCO(CH2)n— where n is an integer of 1 to 5, E is a connecting bond, O, or a methylene, X is OH or H provided that when E is O or a methylene, X is not H, and Y and Z are independently H, a halogen, an alkoxy, or an alkyl optionally substituted with a halogen.Type: GrantFiled: March 20, 1998Date of Patent: September 24, 2002Assignee: Suntory LimitedInventors: Hirokazu Annoura, Kyoko Nakanishi, Shigeki Tamura
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Publication number: 20020133013Abstract: A process for the preparation of trifluoroethoxy benzoic acid derivatives, in particular Flecainide, and their pharmaceutically acceptable salts, starting with commercially available halobenzoic acids and involving the use of simple reagents and low cost solvents, to afford high overall yield of the product.Type: ApplicationFiled: July 23, 2001Publication date: September 19, 2002Applicant: FineTech Ltd.Inventors: Arie L. Gutman, Genady Nisnevich, Eleonora Shkolnik, Igor Zaltzman, Boris Tishin
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Patent number: 6451791Abstract: An amidoaromatic ring sulfonamide hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed, as are a treatment process that comprises administering a contemplated amidoaromatic ring sulfonamide hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.Type: GrantFiled: June 4, 1999Date of Patent: September 17, 2002Assignee: Monsanto CompanyInventors: Robert M. Heintz, Daniel P. Getman, Joseph J. McDonald, Gary A. DeCrescenzo, Susan C. Howard, S. Zaheer Abbas
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Publication number: 20020123493Abstract: The present invention relates to cyclic amine derivatives for treating or preventing neuronal damage associated with neurological diseases. The invention also provides compositions comprising the compounds of the present invention and methods of utilizing those compositions for treating or preventing neuronal damage.Type: ApplicationFiled: January 3, 2002Publication date: September 5, 2002Inventors: Michael Mullican, David Lauffer
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Patent number: 6444686Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.Type: GrantFiled: December 17, 1999Date of Patent: September 3, 2002Assignee: Brsitol-Myers Squibb Pharma CompanyInventors: Soo S. Ko, George V. DeLucca, John V. Duncia, Ui Tae Kim, Joseph B. Santella, III, Dean A. Wacker
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Publication number: 20020107241Abstract: The present invention relates N-heterocyclic derivatives for treating or preventing neuronal damage associated with neurological diseases. The invention also provides compositions comprising the compounds of the present invention and methods of utilizing those compositions for treating or preventing neuronal damage.Type: ApplicationFiled: January 3, 2002Publication date: August 8, 2002Inventors: David Lauffer, Brian Ledford, Michael Mullican
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Publication number: 20020103205Abstract: Di-N-substituted piperazine or 1,4 di-substituted piperadine compounds in accordance with formula I (including all isomers, salts, esters, and solvates) 1Type: ApplicationFiled: July 11, 2001Publication date: August 1, 2002Inventors: Derek Lowe, Wei Chang, Joseph Kozlowski, Joel G. Berger, Robert McQuade, Allen Barnett, Margaret Sherlock, Wing Tom, Sundeep Dugar, Lian-Yong Chen, John W. Clader, Samuel Chackalamannil, Wang Yuguang, Stuart W. McCombie, Jayaram R. Tagat, Susan F. Vice, Wayne Vaccaro, Michael J. Green, Margaret E. Browne, Theodros Asberom
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Publication number: 20020099218Abstract: Compounds and methods of preparing compounds of the formula:Type: ApplicationFiled: October 25, 2001Publication date: July 25, 2002Inventors: Thomas P. Sassi, Ram B. Gupta
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Patent number: 6423689Abstract: The present invention provides compounds that block calcium channels having the Formula I shown below. The present invention also provides methods of using the compounds of Formula I to treat stroke, cerebral ischemia, head trauma, or epilepsy and to pharmaceutical compositions that contain the compounds of Formula I.Type: GrantFiled: December 16, 1998Date of Patent: July 23, 2002Assignees: Warner-Lambert Company, Neurex CorporationInventors: Richard John Booth, Louis Brogley, Wayne Livingston Cody, David Thomas Connor, Harriet Wall Hamilton, John Xiaoqiang He, Lain-Yen Hu, Leonard Joseph Lescosky, Thomas Charles Malone, Laszlo Nadasdi, Michael Francis Rafferty, Bruce David Roth, Diego F. Silva, Yuntao Song, Balazs G. Szoke, Laszlo Urge
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Patent number: 6410566Abstract: A compound represented by the general formula (I), a pharmaceutically acceptable acid addition salt thereof or a pharmaceutically acceptable C1-C6 alkyl addition salt thereof, and their medical applications. These compounds inhibit the action of chemokines such as MIP-1&agr; and/or MCP-1 on target cells, and are useful as therapeutic and/or preventative drugs in diseases, such as atherosclerosis, rheumatoid arthritis, and the like where blood monocytes and lymphocytes infiltrate into tissues.Type: GrantFiled: July 16, 2001Date of Patent: June 25, 2002Assignees: Teijin Limited, Dupont Phamaceuticals CompanyInventors: Tatsuki Shiota, Ken-ichiro Kataoka, Minoru Imai, Takaharu Tsutsumi, Masaki Sudoh, Ryo Sogawa, Takuya Morita, Takahiko Hada, Yumiko Muroga, Osami Takenouchi, Minoru Furuya, Noriaki Endo, Christine M. Tarby, Wilna Moree, Steven Teig
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Publication number: 20020049329Abstract: Compounds of formula (I), a method for obtaining them and pharmaceutical compositions containing them are described. The compounds are useful as human NK3 receptor antagonists.Type: ApplicationFiled: September 18, 2001Publication date: April 25, 2002Inventors: Bichon Daniel, Emonds-Alt Xavier, Gueule Patrick, Proietto Vincenzo, Van Broeck Didier
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Publication number: 20020045626Abstract: Disclosed are compounds of the formula: 1Type: ApplicationFiled: October 11, 2001Publication date: April 18, 2002Applicant: Neurogen CorporationInventors: Renata Xavier Kover, Silva Terdjanian, Jennifer Tran, Andrew Thurkauf
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Publication number: 20020035263Abstract: Compounds of the formula 1Type: ApplicationFiled: September 18, 2001Publication date: March 21, 2002Applicant: American Home Products CorporationInventors: Michael G. Kelly, Gan Zhang, Yvette L. Palmer, Wayne E. Childers
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Patent number: 6359139Abstract: Synthetic methods are provided comprising the steps of racemizing l-threo-piperidyl acetamides to form a mixture of d-threo, l-threo, d-erythro, and l-erythro-piperidyl acetamides by reacting said l-threo-piperidyl acetamides with alkanoic acid.Type: GrantFiled: November 7, 2000Date of Patent: March 19, 2002Assignee: Celgene CorporationInventors: Vikram Khetani, William Konnecke, Chuansheng Ge
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Publication number: 20020032218Abstract: Compounds of formula I activate the insulin receptor kinase. Pharmaceutical compositions comprising the compounds, and methods of treatment of hyperglycemia and other diseases involving imbalance of glucose levels, especially for the treatment of type II diabetes, by administering these compounds to mannnalian hosts, and processes for their preparation, are also described.Type: ApplicationFiled: May 31, 2001Publication date: March 14, 2002Inventors: John Patterson, Sophia Jeong-Weon Park, Robert T. Lum, Wayne R. Spevak
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Publication number: 20020019536Abstract: The present invention relates to urethanes and the thio and dithio analogues thereof of general formula 1Type: ApplicationFiled: March 24, 1999Publication date: February 14, 2002Inventors: ROLAND MAIER, RUDOLF HURNAUS, MICHAEL MARK, BERNHARD EISELE, PETER MUELLER, GEBHARD ADELGOSS, GEBHARD SCHILCHER
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Patent number: 6342508Abstract: Matrix metalloproteinases (MMps) are a group of enzymes that have been implicated in the pathological destruction of connective tissue and basement membranes. These zinc containing endopeptidases consist of several subsets of enzymes including collagenases, stromelysins and gelatinases. TNF-&agr; converting enzyme (TACE), a pro-inflammatory cytokine, catalyzes the formation of TNF-&agr; from membrane bound TNF-&agr; precursor protein. It is expected that small molecule inhibitors of MMPs and TACE therefore have the potential for treating a variety of disease states. The present invention provides low molecular weight, non-peptide inhibitors of matrix metalloproteinases (MMPs) and TNF-&agr; converting enzyme (TACE) for the treatment of arthritis, tumor metastasis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, diabetes (insulin resistance) and HIV infection.Type: GrantFiled: August 17, 2000Date of Patent: January 29, 2002Assignee: American Cyanamid CompanyInventors: Aranapakam Mudumbai Venkatesan, George Theodore Grosu, Jamie Marie Davis, Derek Cecil Cole
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Patent number: 6342509Abstract: This invention relates to certain piperidine quatemrwy salts of Formula (I): that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.Type: GrantFiled: November 18, 1999Date of Patent: January 29, 2002Assignee: Syntex (U.S.A.) LLCInventors: Donald Roy Hirschfeld, Denis John Kertesz, David Berard Smith
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Patent number: 6337398Abstract: Succinoylamino hydroxyethylamino sulfonyl urea derivatives of the formula: wherein the substituents are as defined in the specification, are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: October 13, 1995Date of Patent: January 8, 2002Assignee: G.D. Searle & Co.Inventors: Michael L Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
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Publication number: 20010056185Abstract: Novel C3A ligands are provided. Methods of using the present compounds to treat immune and inflammation disease are also provided.Type: ApplicationFiled: March 12, 2001Publication date: December 27, 2001Inventor: Dennis Lee
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Publication number: 20010053851Abstract: Para-alkynyl phenyl heteroaromatic amides which are active as glucokinase activators to increase insulin secretion which makes them useful for treating type II diabetes.Type: ApplicationFiled: April 25, 2001Publication date: December 20, 2001Inventor: Paige E. Mahaney
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Patent number: 6331507Abstract: There is disclosed substituted thiocarboxamides of the general formula (I) useful as herbicides.Type: GrantFiled: December 22, 1999Date of Patent: December 18, 2001Assignee: Bayer AktiengesellschaftInventors: Karl-Heinz Linker, Kurt Findeisen, Roland Andree, Mark-Wilhelm Drewes, Andreas Lender, Otto Schallner, Wilhelm Haas, Hans-Joachim Santel, Markus Dollinger
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Patent number: 6319920Abstract: This invention relates to muscarinic receptor antagonist compounds selected from the group of compounds represented by Formula I: wherein the substituents are as defined in the specification; and their pharmaceutically acceptable salts, individual isomers or a racemic or non-racemic mixture; pharmaceutical compositions containing them; and methods for their use as therapeutic agents.Type: GrantFiled: February 1, 1999Date of Patent: November 20, 2001Assignee: Syntex (U.S.A.) LLCInventors: Joan Marie Caroon, Robin Douglas Clark, Michael Patrick Dillon, Ralph New Harris, III, Sharathchandra Surendra Hegde, Clara Jeou Jen Lin, Hans Maag, David Bruce Repke
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Patent number: 6316627Abstract: A process for the preparation of trifluoroethoxy benzoic acid derivatives, in particular Flecainide, and their pharmaceutically acceptable salts, starting with commercially available halobenzoic acids and involving the use of simple reagents and low cost solvents, to afford high overall yield of the product. The above object is achieved in accordance with the present invention which, in one aspect thereof, provides a process for preparing a compound of formula (A): and pharmaceutically acceptable salts thereof, which process comprises the steps of: a) reacting a halobenzoic acid or a salt thereof of the formula [II ] with 2,2,2-trifluoroethanol in the presence of a strong base and a copper containing material, if desired followed by acidification to obtain a compound of formula [I] b) converting the product obtained in step a) above into the compound of formula (A) or a pharmaceutically acceptable salt thereof.Type: GrantFiled: October 21, 1999Date of Patent: November 13, 2001Assignee: Fine Tech Ltd.Inventors: Arie L. Gutman, Genady Nisnevich, Eleonora Shkolnik, Igor Zaltzman, Boris Tishin
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Patent number: 6313097Abstract: Compounds of the formula (I) wherein A, R, R1, R2, X1, X2, X3, and Y are as defined herein, and the tautomers and the pharmaceutically acceptable salts thereof, including pharmaceutical compositions containing these compounds, and their use in the selective antagonization of calcitonin gene-related peptide (CGRP) and in the treatment or prophylaxis of migraine or cluster headaches, non-insulin-dependent diabetes mellitus, inflammation, allergic rhinitis, asthma, morphine tolerance, menopausal hot flashes, and diseases characterized by excessive vasodilatation and consequent reduction in blood-flow.Type: GrantFiled: March 10, 2000Date of Patent: November 6, 2001Assignee: Boehringer Ingelheim Pharma KGInventors: Wolfgang Eberlein, Klaus Rudolf, Wolfhard Engel, Henri Doods, Gerhard Hallermayer
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Patent number: 6306859Abstract: Compounds of the Formula (I) wherein R2, Y, X and n are as defined in the specification which compounds are useful in the treatment of disorders associated with serotonergic neuron-related diseases.Type: GrantFiled: March 1, 2000Date of Patent: October 23, 2001Assignee: American Home Products CorporationInventors: Wayne E. Childers, Michael G. Kelly, Gan Zhang, Yvette L. Palmer, Edward J. Podlesny
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Publication number: 20010006619Abstract: The present invention relates to a class of compounds having affinity for certain cancer cells, e.g. lung carcinomas, colon carcinomas, renal carcinomas, prostate carcinomas, breast carcinomas, malignant melanomas, gliomas, neuroblastomas and pheochromocytomas. The compounds of the present invention can also bind with high specificity to cell surface sigma receptors and can therefore be used for diagnostic imaging of any tissue having an abundance of cells with sigma receptors. The present invention provides such compounds as agents for diagnostic imaging and for detecting and treating tumors containing the cancer cells described above.Type: ApplicationFiled: January 5, 2001Publication date: July 5, 2001Applicant: RESEARCH CORPORATION TECHNOLOGIES, INC.Inventors: Christy S. John, Jesse Baumgold, John G. McAfee, Terry Moody, Wayne Bowen
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Patent number: 6255301Abstract: There is provided compounds of formula I, wherein R1, R2, R3, Rx, Y, n and B have meanings given in the description which are useful as competitive inhibitors of trypsin-like proteases, such as thrombin, and in particular in the treatment of conditions where inhibition of thrombin is required as in thrombosis or as anticoagulants.Type: GrantFiled: July 14, 1997Date of Patent: July 3, 2001Assignee: AstraZeneca ABInventors: David Gustafsson, Jan-Erik Nyström
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Patent number: 6248304Abstract: This invention provides scintigraphic imaging agents and reagents for preparing said agents, methods for radiolabeling said reagents and kits containing non-radioactive reagents and other components for the convenient preparation of the scintigraphic imaging agents. More specifically, the invention provides scintigraphic imaging agents that are radiolabeled compounds which bind with high affinity to GPIIb/IIIa receptors on activated platelets and using such radiolabeled compounds derivatives to image sites in a mammalian body.Type: GrantFiled: September 27, 1996Date of Patent: June 19, 2001Assignee: Berlex Laboratories, Inc.Inventors: John Lister-James, Richard T. Dean
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Patent number: 6242466Abstract: Phenylamidines of the formula (I) wherein: R6 is a C5-12-alkyloxycarbonyl group, and R7 is a hydrogen atom, or a C1-8-alkyl, C4-7-cycloalkyl, phenyl-C1-4-alkyl, or R8—CO—OCHR9— group, wherein R8 is a C1-4-alkyl, C1-4-alkoxy, C3-7-cycloalkyl, or C4-7-cycloalkoxy group, and R9 is a hydrogen atom or a C1-4-alkyl group, or a tautomer or pharmaceutically acceptable salt thereof. These compounds inhibit cell aggregation and are useful for the treatment or prevention of thrombosis, inflammation, bone degradation, tumors and tumor metastasis.Type: GrantFiled: July 14, 1999Date of Patent: June 5, 2001Assignee: Boehringer Ingelheim Pharma KGInventors: Frank Himmelsbach, Brian Guth, Hans-Dieter Schubert
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Patent number: 6218389Abstract: The invention provides compounds of formula as described in the claims, or an optical isomer, diastereomer or enantiomer thereof, or a pharmaceutically-acceptable salt, or biohydrolyzable amide, ester, or imide thereof are useful as inhibitors of metalloproteases. Also disclosed are pharmaceutical compositions and methods of treating diseases, disorders and conditions characterized by metalloprotease activity using these compounds or the pharmaceutical compositions containing them.Type: GrantFiled: July 31, 1998Date of Patent: April 17, 2001Assignee: The Procter & Gamble Co.Inventors: Neil Gregory Almstead, Roger Gunnard Bookland, Yetunde Olabisi Taiwo, Rimma Sandler Bradley, Rodney Dean Bush, Biswanath De, Michael George Natchus, Stanislaw Pikul
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Patent number: 6180759Abstract: This invention is directed to a process for preparing a pseudotetrapeptide of formula I or a salt or prodrug thereof wherein is optionally nitrogen protected azaheterocyclyl; is a single or double bond; q is 1-5; B is alkyl, cycloalkyl, cycloalkylalkyl, alkylcycloalkyl, alkylcycloalkylalkyl, aryl, aralkyl, alkylaryl, or alkylaralkyl; Q2 is H or a carboxylic acid protecting group; J is —H, alkyl, cycloalkyl, cycloalkylalkyl, alkylcycloalkyl, alkylcycloalkylalkyl, aryl, substituted aryl, aralkyl, substituted aralkyl; L is OR1, or NR1R2, where R1 and R2 are independently —H, alkyl, cycloalkyl, cycloalkylalkyl, alkylcycloalkyl, alkylcycloalkylalkyl, aryl, aralkyl, alkylaryl or alkylaralkyl; and p is 1 or 2 which comprises the coupling of two dipeptides or psuedopeptides.Type: GrantFiled: April 7, 2000Date of Patent: January 30, 2001Assignee: Aventis Pharmaceuticals Products Inc.Inventors: James J. Mencel, Robert Stammler, Christophe Daubie, Michel Lavigne, Benoit J. Vanasse, Robert C. Liu, Patrick Leon, Geoffrey A. D'Netto, Adam W. Sledeski
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Patent number: 6174885Abstract: A [6-(substituted-methyl)-3-cyclohexenyl]formamide derivative or a salt thereof expressed by the following Formula (I): wherein one of A and B is a hydrocarbon group of C10-30 expressed by R1 and the other is—(CH2)n-NR2R3; Z is —O—, —OCO—, —OCONR6— or —NR6—; R2 and R3 individually represent a hydrogen, lower alkyl, phenyl or benzyl group, or together represent a heterocycle having 3-7 members; —NR5—(CH2)n-NR2R3 or —NR6—(CH2)n-NR2R3 may be Group W, and —OCONR6—(CH2)n-NR2R3 may be —OCO—W, wherein W is a formula of: wherein ring E is a heterocycle of 6 or 7 members including two nitrogen atoms and R2 is a hydrogen, lower alkyl, phenyl or benzyl group; R4 is a halogen, lower alkyl, lower acyl, nitro, cyano, lower alkoxycarbonyl, carbamoyl, lower alkylcarbamoyl, lower alkylamino, lower acylamino, lower alkoxy or lower acyloxy group; each of R5 and R6 is a hydrogen, lowType: GrantFiled: February 26, 1999Date of Patent: January 16, 2001Assignee: Shiseido Co., Ltd.Inventors: Hirotada Fukunishi, Tsunao Magara, Koji Kobayashi
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Patent number: 6162919Abstract: A process for preparing the d-threo isomer of methylphenidate hydrochloride comprising converting d,l-threo methylphenidate hydrochloride to the free base form in a first step, resolving the free base prepared in the first step with (R)-(-)-1,1'-binaphthyl-2,2'-diyl hydrogen phosphate to obtain the phosphate salt enriched with the d-threo isomer of methylphenidate in a second step, basifying the phosphate salt to obtain the free base form of the d-threo isomer of methylphenidate in a third step, converting the free base to the hydrochloride salt form of the d-threo isomer of methylphenidate in high optical purity in a fourth step, and recrystallizing the hydrochloride salt form to obtain the desired d-threo isomer in a higher optical purity. An alternative embodiment relates to the preparation of the d-threo isomer of methylphenidate hydrochloride utilizing the hydrochloride salt form of the racemic mixture of threo-methylphenidate directly.Type: GrantFiled: December 3, 1998Date of Patent: December 19, 2000Assignee: Novartis AGInventors: Mahavir Prashad, Bin Hu
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Patent number: 6159989Abstract: There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.Type: GrantFiled: December 15, 1999Date of Patent: December 12, 2000Assignee: Merck & Co., Inc.Inventors: Lin Chu, Mark Goulet, Thomas F. Walsh, Matthew J. Wyvratt, Stephanie L. Witkin
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Patent number: 6156768Abstract: Certain Alpha- and Beta-amino acid hydroxyethylamino sulfamic acid derivatives represented by the following formula are useful as retroviral protease inhibitors: ##STR1##Type: GrantFiled: February 2, 1995Date of Patent: December 5, 2000Assignee: G. D. Searle & Co.Inventors: Michael L Vazquez, Richard A Mueller, John J Talley, Daniel P Getman, Gary A DeCrescenzo, Eric T Sun
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Patent number: 6156900Abstract: A process for the preparation of optically-enriched pipecolic acid as a salt with an optically-active acid, comprises asymmetric transformation of pipecolic acid, as a racemic mixture of a mixture enriched in the opposite enantiomer from that desired, with the optically-active acid in a solvent comprising an acid that causes racemisation, in the absence of aldehyde.Type: GrantFiled: February 12, 1999Date of Patent: December 5, 2000Assignee: Darwin Discovery LimitedInventors: Ulrich Conrad Dyer, Martin Woods, Raymond McCague
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Patent number: 6143744Abstract: This invention relates to sulfamides of formula (I) ##STR1## that are inhibitors of metalloproteases, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.Type: GrantFiled: August 5, 1999Date of Patent: November 7, 2000Assignees: Syntex (U.S.A.) Inc., Agouron Pharmaceuticals, Inc.Inventors: Chris Allen Broka, Jeffrey Allen Campbell, Arlindo Lucas Castelhano, Jian Jeffrey Chen, Robert Than Hendricks, Michael Joseph Melnick, Keith Adrian Murray Walker