Acyclic Nitrogen Bonded Directly To A -c(=x)- Group, Wherein X Is Chalcogen Patents (Class 546/233)
  • Patent number: 6509356
    Abstract: 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: Grant
    Filed: August 4, 1998
    Date of Patent: January 21, 2003
    Assignee: Eli Lilly and Company
    Inventors: Jeffrey Alan Dodge, Andrew Lawrence Glasebrook, Charles Willis Lugar, III
  • Patent number: 6500823
    Abstract: 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: Grant
    Filed: March 2, 2001
    Date of Patent: December 31, 2002
    Assignee: N-Gene Research Laboratories, Inc.
    Inventors: Péter Literáti Nagy, Kálmán Takács, Balázs Sümegi
  • Publication number: 20020193634
    Abstract: 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: Application
    Filed: May 22, 2002
    Publication date: December 19, 2002
    Inventors: Zixia Feng, Mark R. Hellberg, Steven T. Miller
  • Publication number: 20020193602
    Abstract: The present application relates to novel opioid receptor antagonists and agonists, methods of making these compounds, and methods of use thereof.
    Type: Application
    Filed: March 19, 2002
    Publication date: December 19, 2002
    Applicant: Research Triangle Institute
    Inventors: Frank I. Carroll, James B. Thomas, S. Wayne Mascarella
  • Publication number: 20020169324
    Abstract: The present application relates to novel opioid receptor antagonists and agonists, methods of making these compounds, and methods of use thereof.
    Type: Application
    Filed: March 19, 2002
    Publication date: November 14, 2002
    Applicant: Research Triangle Institute
    Inventors: Frank I. Carroll, James B. Thomas, S. Wayne Mascarella
  • Patent number: 6479502
    Abstract: 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: Grant
    Filed: February 21, 2001
    Date of Patent: November 12, 2002
    Assignee: British Biotech Pharmaceuticals
    Inventor: Fionna Mitchell Martin
  • Publication number: 20020165396
    Abstract: The present application relates to novel opioid receptor antagonists and agonists, methods of making these compounds, and methods of use thereof.
    Type: Application
    Filed: March 19, 2002
    Publication date: November 7, 2002
    Applicant: Research Triangle Institute
    Inventors: Frank I. Carroll, James B. Thomas, S. Wayne Mascarella
  • Patent number: 6476027
    Abstract: 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: Grant
    Filed: December 6, 1999
    Date of Patent: November 5, 2002
    Assignee: Monsanto Company
    Inventors: 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
  • Patent number: 6472394
    Abstract: 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 tr
    Type: Grant
    Filed: December 17, 2001
    Date of Patent: October 29, 2002
    Assignee: Schering Corporation
    Inventors: Brian A. McKittrick, Jing Su, John W. Clader, Shengjian Li, Guihau Guo
  • Publication number: 20020151534
    Abstract: Antithrombotic compounds of general formula 1
    Type: Application
    Filed: January 16, 2002
    Publication date: October 17, 2002
    Inventors: Uwe Joerg Ries, Henning Priepke, Herbert Nar, Jean-Marie Stassen, Wolfgang Wienen
  • Patent number: 6465468
    Abstract: 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: Grant
    Filed: March 22, 2000
    Date of Patent: October 15, 2002
    Assignee: Darwin Discovery Limited
    Inventors: Andrew Douglas Baxter, David Alan Owen, Duncan Batty, Robert John Watson
  • Patent number: 6458957
    Abstract: 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: Grant
    Filed: July 12, 2000
    Date of Patent: October 1, 2002
    Assignee: Geneva Pharmaceuticals, Inc.
    Inventors: Anup K. Ray, Hiren Patel, Shilpa V. Merai, Mahendra R. Patel
  • Patent number: 6455549
    Abstract: 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: Grant
    Filed: March 20, 1998
    Date of Patent: September 24, 2002
    Assignee: Suntory Limited
    Inventors: Hirokazu Annoura, Kyoko Nakanishi, Shigeki Tamura
  • Publication number: 20020133013
    Abstract: 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: Application
    Filed: July 23, 2001
    Publication date: September 19, 2002
    Applicant: FineTech Ltd.
    Inventors: Arie L. Gutman, Genady Nisnevich, Eleonora Shkolnik, Igor Zaltzman, Boris Tishin
  • Patent number: 6451791
    Abstract: 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: Grant
    Filed: June 4, 1999
    Date of Patent: September 17, 2002
    Assignee: Monsanto Company
    Inventors: Robert M. Heintz, Daniel P. Getman, Joseph J. McDonald, Gary A. DeCrescenzo, Susan C. Howard, S. Zaheer Abbas
  • Publication number: 20020123493
    Abstract: 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: Application
    Filed: January 3, 2002
    Publication date: September 5, 2002
    Inventors: Michael Mullican, David Lauffer
  • Patent number: 6444686
    Abstract: 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: Grant
    Filed: December 17, 1999
    Date of Patent: September 3, 2002
    Assignee: Brsitol-Myers Squibb Pharma Company
    Inventors: Soo S. Ko, George V. DeLucca, John V. Duncia, Ui Tae Kim, Joseph B. Santella, III, Dean A. Wacker
  • Publication number: 20020107241
    Abstract: 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: Application
    Filed: January 3, 2002
    Publication date: August 8, 2002
    Inventors: David Lauffer, Brian Ledford, Michael Mullican
  • Publication number: 20020103205
    Abstract: Di-N-substituted piperazine or 1,4 di-substituted piperadine compounds in accordance with formula I (including all isomers, salts, esters, and solvates) 1
    Type: Application
    Filed: July 11, 2001
    Publication date: August 1, 2002
    Inventors: 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
  • Publication number: 20020099218
    Abstract: Compounds and methods of preparing compounds of the formula:
    Type: Application
    Filed: October 25, 2001
    Publication date: July 25, 2002
    Inventors: Thomas P. Sassi, Ram B. Gupta
  • Patent number: 6423689
    Abstract: 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: Grant
    Filed: December 16, 1998
    Date of Patent: July 23, 2002
    Assignees: Warner-Lambert Company, Neurex Corporation
    Inventors: 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
  • Patent number: 6410566
    Abstract: 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: Grant
    Filed: July 16, 2001
    Date of Patent: June 25, 2002
    Assignees: Teijin Limited, Dupont Phamaceuticals Company
    Inventors: 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
  • Publication number: 20020049329
    Abstract: 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: Application
    Filed: September 18, 2001
    Publication date: April 25, 2002
    Inventors: Bichon Daniel, Emonds-Alt Xavier, Gueule Patrick, Proietto Vincenzo, Van Broeck Didier
  • Publication number: 20020045626
    Abstract: Disclosed are compounds of the formula: 1
    Type: Application
    Filed: October 11, 2001
    Publication date: April 18, 2002
    Applicant: Neurogen Corporation
    Inventors: Renata Xavier Kover, Silva Terdjanian, Jennifer Tran, Andrew Thurkauf
  • Publication number: 20020035263
    Abstract: Compounds of the formula 1
    Type: Application
    Filed: September 18, 2001
    Publication date: March 21, 2002
    Applicant: American Home Products Corporation
    Inventors: Michael G. Kelly, Gan Zhang, Yvette L. Palmer, Wayne E. Childers
  • Patent number: 6359139
    Abstract: 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: Grant
    Filed: November 7, 2000
    Date of Patent: March 19, 2002
    Assignee: Celgene Corporation
    Inventors: Vikram Khetani, William Konnecke, Chuansheng Ge
  • Publication number: 20020032218
    Abstract: 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: Application
    Filed: May 31, 2001
    Publication date: March 14, 2002
    Inventors: John Patterson, Sophia Jeong-Weon Park, Robert T. Lum, Wayne R. Spevak
  • Publication number: 20020019536
    Abstract: The present invention relates to urethanes and the thio and dithio analogues thereof of general formula 1
    Type: Application
    Filed: March 24, 1999
    Publication date: February 14, 2002
    Inventors: ROLAND MAIER, RUDOLF HURNAUS, MICHAEL MARK, BERNHARD EISELE, PETER MUELLER, GEBHARD ADELGOSS, GEBHARD SCHILCHER
  • Patent number: 6342508
    Abstract: 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: Grant
    Filed: August 17, 2000
    Date of Patent: January 29, 2002
    Assignee: American Cyanamid Company
    Inventors: Aranapakam Mudumbai Venkatesan, George Theodore Grosu, Jamie Marie Davis, Derek Cecil Cole
  • Patent number: 6342509
    Abstract: 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: Grant
    Filed: November 18, 1999
    Date of Patent: January 29, 2002
    Assignee: Syntex (U.S.A.) LLC
    Inventors: Donald Roy Hirschfeld, Denis John Kertesz, David Berard Smith
  • Patent number: 6337398
    Abstract: 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: Grant
    Filed: October 13, 1995
    Date of Patent: January 8, 2002
    Assignee: G.D. Searle & Co.
    Inventors: Michael L Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
  • Publication number: 20010056185
    Abstract: Novel C3A ligands are provided. Methods of using the present compounds to treat immune and inflammation disease are also provided.
    Type: Application
    Filed: March 12, 2001
    Publication date: December 27, 2001
    Inventor: Dennis Lee
  • Publication number: 20010053851
    Abstract: 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: Application
    Filed: April 25, 2001
    Publication date: December 20, 2001
    Inventor: Paige E. Mahaney
  • Patent number: 6331507
    Abstract: There is disclosed substituted thiocarboxamides of the general formula (I) useful as herbicides.
    Type: Grant
    Filed: December 22, 1999
    Date of Patent: December 18, 2001
    Assignee: Bayer Aktiengesellschaft
    Inventors: Karl-Heinz Linker, Kurt Findeisen, Roland Andree, Mark-Wilhelm Drewes, Andreas Lender, Otto Schallner, Wilhelm Haas, Hans-Joachim Santel, Markus Dollinger
  • Patent number: 6319920
    Abstract: 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: Grant
    Filed: February 1, 1999
    Date of Patent: November 20, 2001
    Assignee: Syntex (U.S.A.) LLC
    Inventors: 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
  • Patent number: 6316627
    Abstract: 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: Grant
    Filed: October 21, 1999
    Date of Patent: November 13, 2001
    Assignee: Fine Tech Ltd.
    Inventors: Arie L. Gutman, Genady Nisnevich, Eleonora Shkolnik, Igor Zaltzman, Boris Tishin
  • Patent number: 6313097
    Abstract: 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: Grant
    Filed: March 10, 2000
    Date of Patent: November 6, 2001
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Wolfgang Eberlein, Klaus Rudolf, Wolfhard Engel, Henri Doods, Gerhard Hallermayer
  • Patent number: 6306859
    Abstract: 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: Grant
    Filed: March 1, 2000
    Date of Patent: October 23, 2001
    Assignee: American Home Products Corporation
    Inventors: Wayne E. Childers, Michael G. Kelly, Gan Zhang, Yvette L. Palmer, Edward J. Podlesny
  • Publication number: 20010006619
    Abstract: 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: Application
    Filed: January 5, 2001
    Publication date: July 5, 2001
    Applicant: RESEARCH CORPORATION TECHNOLOGIES, INC.
    Inventors: Christy S. John, Jesse Baumgold, John G. McAfee, Terry Moody, Wayne Bowen
  • Patent number: 6255301
    Abstract: 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: Grant
    Filed: July 14, 1997
    Date of Patent: July 3, 2001
    Assignee: AstraZeneca AB
    Inventors: David Gustafsson, Jan-Erik Nyström
  • Patent number: 6248304
    Abstract: 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: Grant
    Filed: September 27, 1996
    Date of Patent: June 19, 2001
    Assignee: Berlex Laboratories, Inc.
    Inventors: John Lister-James, Richard T. Dean
  • Patent number: 6242466
    Abstract: 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: Grant
    Filed: July 14, 1999
    Date of Patent: June 5, 2001
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Frank Himmelsbach, Brian Guth, Hans-Dieter Schubert
  • Patent number: 6218389
    Abstract: 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: Grant
    Filed: July 31, 1998
    Date of Patent: April 17, 2001
    Assignee: 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
  • Patent number: 6180759
    Abstract: 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: Grant
    Filed: April 7, 2000
    Date of Patent: January 30, 2001
    Assignee: 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
  • Patent number: 6174885
    Abstract: 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, low
    Type: Grant
    Filed: February 26, 1999
    Date of Patent: January 16, 2001
    Assignee: Shiseido Co., Ltd.
    Inventors: Hirotada Fukunishi, Tsunao Magara, Koji Kobayashi
  • Patent number: 6162919
    Abstract: 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: Grant
    Filed: December 3, 1998
    Date of Patent: December 19, 2000
    Assignee: Novartis AG
    Inventors: Mahavir Prashad, Bin Hu
  • Patent number: 6159989
    Abstract: 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: Grant
    Filed: December 15, 1999
    Date of Patent: December 12, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Lin Chu, Mark Goulet, Thomas F. Walsh, Matthew J. Wyvratt, Stephanie L. Witkin
  • Patent number: 6156768
    Abstract: Certain Alpha- and Beta-amino acid hydroxyethylamino sulfamic acid derivatives represented by the following formula are useful as retroviral protease inhibitors: ##STR1##
    Type: Grant
    Filed: February 2, 1995
    Date of Patent: December 5, 2000
    Assignee: G. D. Searle & Co.
    Inventors: Michael L Vazquez, Richard A Mueller, John J Talley, Daniel P Getman, Gary A DeCrescenzo, Eric T Sun
  • Patent number: 6156900
    Abstract: 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: Grant
    Filed: February 12, 1999
    Date of Patent: December 5, 2000
    Assignee: Darwin Discovery Limited
    Inventors: Ulrich Conrad Dyer, Martin Woods, Raymond McCague
  • Patent number: 6143744
    Abstract: 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: Grant
    Filed: August 5, 1999
    Date of Patent: November 7, 2000
    Assignees: 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