Chalcogen Attached Indirectly To The Five-membered Hetero Ring By Acyclic Nonionic Bonding Patents (Class 548/562)
  • Publication number: 20080194581
    Abstract: The invention concerns compounds of formula (I): Wherein R1, R2, R3, R4, R5, R6, R7, R8 and R9 are as defined herein. The invention also concerns the method for preparing said compounds including the intermediates therefor and their therapeutic use.
    Type: Application
    Filed: April 14, 2008
    Publication date: August 14, 2008
    Applicant: SANOFI-AVENTIS
    Inventors: Francis BARTH, Christian CONGY, Laurent HORTALA, Murielle RINALDI-CARMONA
  • Publication number: 20080188402
    Abstract: The present invention relates to novel substituted pyrrole compounds, their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them. This invention particularly relates to novel substituted pyrrole compounds of the general formula (I), their analogs, their derivatives, their polymorphs, their tautomeric forms, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and their pharmaceutical compositions containing them. This invention also relates to the process for preparing such compounds, a composition containing such a compound and the use of such a compound and composition in medicine.
    Type: Application
    Filed: January 23, 2008
    Publication date: August 7, 2008
    Applicant: Cadilla Healthcare Limited
    Inventors: Braj Bhushan LOHRAY, Vidya Bhushan Lohray, Vijay Kumar Gajubhai Barot
  • Publication number: 20080167480
    Abstract: The present invention relates to an improved synthesis of pyrrole capping group precursors.
    Type: Application
    Filed: June 13, 2007
    Publication date: July 10, 2008
    Inventor: Michael Wallace
  • Patent number: 7323491
    Abstract: The present invention relates to novel substituted pyrrole compounds, their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them. This invention particularly relates to novel substituted pyrrole compounds of the general formula (I), their analogs, their derivatives, their polymorphs, their tautomeric forms, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and their pharmaceutical compositions containing them This invention also relates to the process for preparing such compounds, a composition containing such a compound and the use of such a compound and composition in medicine.
    Type: Grant
    Filed: March 1, 2004
    Date of Patent: January 29, 2008
    Assignee: Cadila Healthcare Limited
    Inventors: Braj Bhushan Lohray, Vidya Bhushan Lohray, Vijay Kumar Gajubhai Barot
  • Patent number: 7319152
    Abstract: Compounds of formula I or II are provided, wherein R1-R8 are defined herein, and pharmaceutical compositions and kits containing these compounds.
    Type: Grant
    Filed: September 18, 2006
    Date of Patent: January 15, 2008
    Assignee: Wyeth
    Inventors: Puwen Zhang, Jeffrey Curtis Kern, Eugene Anthony Terefenko, Eugene John Trybulski
  • Patent number: 7250444
    Abstract: HMGCo-A reductase inhibitor compounds useful as hypocholesterolemic and hypolipidemic compounds are provided. Also provided are pharmaceutical compositions of the compounds. Methods of making and methods of using the compounds are also provided.
    Type: Grant
    Filed: June 7, 2004
    Date of Patent: July 31, 2007
    Assignee: Pfizer Inc.
    Inventors: Robert Michael Kennedy, William Keun-Chan Park, Bruce David Roth, Yuntao Song, Bharat K. Trivedi
  • Patent number: 7179581
    Abstract: Resist compositions comprising nitrogen heterocyclic compounds having a pyrrole or nitrogen-bearing 5-membered ring structure and a polar functional group have an excellent resolution and an excellent focus margin and are useful in microfabrication using electron beams or deep-UV light.
    Type: Grant
    Filed: May 20, 2004
    Date of Patent: February 20, 2007
    Assignee: Shin-Etsu Chemical Co., Ltd.
    Inventors: Takeru Watanabe, Jun Hatakeyama
  • Patent number: 7084136
    Abstract: A compound of the formula (I): wherein A is alkylene optionally having an unsaturated bond; R is —C(?O)—R1; R1 is hydroxy or the like; m is 0 or 1; p is 0 or 1; X1 and X3 are each independently optionally substituted aryl or optionally substituted heteroaryl or the like; X2 is a bond, —CH2—, —S—, —SO2—, —CH2—O—, —O—CH2—, —CH2—S—, —S—CH2—, or the like; X4 is —CH2—, —CH2—CH2—, —C(?O)—, or the like, having a dual antagonistic activity against both a thromboxane A2 receptor and a prostaglandin D2 receptor is found.
    Type: Grant
    Filed: May 28, 2001
    Date of Patent: August 1, 2006
    Assignee: Shionogi & Co., Ltd.
    Inventors: Norihiko Tanimoto, Akinori Arimura
  • Patent number: 7041837
    Abstract: Novel ?-aryl-?-substituted propanoic acids having hypolipidemic and hypocholesteremic activities.
    Type: Grant
    Filed: July 19, 2002
    Date of Patent: May 9, 2006
    Assignee: Cadilla Healthcare Limited
    Inventors: Braj Bhushan Lohray, Vidya Bhushan Lohray, Vijay Kumar Gajubhai Barot, Saurin Khimshanker Raval, Preeti Saurin Raval, Sujay Basu
  • Patent number: 7034164
    Abstract: The invention relates to new, inexpensive electropolymers capable of light-induced grafting, onto which specific identification probes can be easily grafted and having optimum capacity for interaction with the target analytes (DNA/DNAc, PNA/PNAc, enzyme/substrate/Antibody/Antigen). These electropolymers capable of light-induced grafting are, for example, poly(pyrrole-benzophenone). Benzophenone forms sites for light-induced grafting. The invention also covers the mono and oligomers which make up these novel electropolymers capable of light-induced grafting. Another object of the invention is the process for their manufacture, as well as electronic biosensors containing these electropolymers capable of being grafted and/or grafted by probes for the analysis of biomolecules.
    Type: Grant
    Filed: August 7, 2000
    Date of Patent: April 25, 2006
    Assignee: Universite Joseph Fourier
    Inventor: Serge Cosnier
  • Patent number: 6987123
    Abstract: The present invention relates to compounds of the general formula (I), there derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, and their pharmaceutically acceptable solvates, wherein all variables are as defined in the specification.
    Type: Grant
    Filed: August 10, 2001
    Date of Patent: January 17, 2006
    Assignee: Cadila Healthcare Limited
    Inventors: Braj Bhushan Lohray, Vidya Bhushan Lohray, Vijay Kumar Gajubhai Barot
  • Patent number: 6924396
    Abstract: The present invention describes immobilized haloenamine reagents, immobilized tertiary amides, methods for their preparation, and methods of use.
    Type: Grant
    Filed: September 17, 2003
    Date of Patent: August 2, 2005
    Assignee: Pharmacia Corporation
    Inventor: Dennis P. Phillion
  • Patent number: 6911468
    Abstract: A compound of the formula (I): wherein X1 and X2 are the same or different and each is a bond or a spacer having 1 to 20 atom(s) in the main chain; one of R1 and R2 is a cycle group having substituent(s) selected from 1) an optionally substituted carboxy-C1-6 alkoxy group and 2) an optionally substituted carboxy-C1-6 aliphatic hydrocarbon group, wherein the cycle group optionally has additional substituent(s), and the other is an optionally substituted cycle group or a hydrogen atom; and R3, R4 and R5 are the same or different and each is a hydrogen atom or a substituent, or R4 may link together with R3 or R5 to form an optionally substituted ring; provided that when R3 is a hydrogen atom, R4 is a hydrogen atom and R5 is methyl, X2—R2 is not 4-cyclohexylphenyl; when R3 is 4-methoxyphenyl, R4 is a hydrogen atom and R5 is methyl, X2—R2 is not 4-methoxyphenyl; and when R1 or R2 is a hydrogen atom, the adjacent X1 or X2 is not a C1-7 alkylene; or a salt thereof exhibits a protein tyrosine phosphatase inhibi
    Type: Grant
    Filed: May 21, 2001
    Date of Patent: June 28, 2005
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Takahiro Matsumoto, Nozomi Katayama, Hiroshi Mabuchi
  • Patent number: 6909003
    Abstract: The invention relates to a process for the manufacture of a compound of formula or a salt, especially a pharmaceutically acceptable salt with a base, thereof or a lactone thereof wherein the element represents —CH2—CH2— or —CH?CH— and R represents a cyclic radical.
    Type: Grant
    Filed: May 2, 2003
    Date of Patent: June 21, 2005
    Assignee: Novartis AG
    Inventor: Thomas Storz
  • Patent number: 6887893
    Abstract: Certain cyclooxygenase-2 inhibitors are useful for the treatment and prevention of tumors and tumor-related disorders and cachexia.
    Type: Grant
    Filed: December 16, 1998
    Date of Patent: May 3, 2005
    Assignee: Sankyo Company, Limited
    Inventors: Shinichi Kurakata, Masaharu Hanai, Saori Kanai, Tomio Kimura
  • Patent number: 6864254
    Abstract: An inhibitor for 20-hydroxyeicosatetraenoic acid production which comprises as the active ingredient a specific hydroxyformamidine derivative or a pharmacologically acceptable salt thereof. It is useful especially as a remedy for kidney diseases, cerebrovascular diseases, or circulatory diseases. The novel hydroxyformamidine derivative or pharmacologically acceptable salt thereof is also provided.
    Type: Grant
    Filed: November 1, 2000
    Date of Patent: March 8, 2005
    Assignee: Taisho Pharmaceutical Co., Ltd.
    Inventors: Masakazu Sato, Noriyuki Miyata, Takaaki Ishii, Yuko Kobayashi, Hideaki Amada
  • Patent number: 6797723
    Abstract: The invention relates to novel heterocycle substituted diphenyl leukotriene B4 (LTB4) antagonists, to compositions containing such compounds, and to methods of using such compounds for treatment of inflammatory diseases.
    Type: Grant
    Filed: April 24, 2002
    Date of Patent: September 28, 2004
    Assignee: Eli Lilly and Company
    Inventors: Jason Scott Sawyer, Douglas Wade Beight, Edward C R Smith, William Thomas McMillen
  • Patent number: 6777559
    Abstract: A process for the preparation heterocyclic indene analogs, especially with the preparation of 4-hydroxycarbazole or N-protected 4-hydroxycarbazole, involves cyclocarbonylation followed by saponification. This process avoids high temperatures and high catalyst loadings.
    Type: Grant
    Filed: January 22, 2002
    Date of Patent: August 17, 2004
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Michelangelo Scalone, Thomas Albert Zeibig
  • Patent number: 6777418
    Abstract: The current invention provide novel retinoid compounds and methods for their synthesis, methods of treating or preventing emphysema, cancer and dermatological disorders and pharmaceutical compositions suitable for the treatment or prevention of emphysema, cancer and dermatological disorders.
    Type: Grant
    Filed: October 1, 2001
    Date of Patent: August 17, 2004
    Assignee: Syntex (U.S.A.) LLC
    Inventors: Jean-Marc Lapierre, David Mark Rotstein, Eric Brian Sjogren
  • Patent number: 6677353
    Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-phenyl-N-heteroaralkyl aminoalcohols.
    Type: Grant
    Filed: May 23, 2002
    Date of Patent: January 13, 2004
    Assignee: Pharmacia Corporation
    Inventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
  • Patent number: 6677487
    Abstract: The present invention describes immobilized haloenamine reagents, immobilized tertiary amides, methods for their preparation, and methods of use.
    Type: Grant
    Filed: February 1, 2002
    Date of Patent: January 13, 2004
    Assignee: Pharmacia Corporation
    Inventor: Dennis P. Phillion
  • Publication number: 20030199498
    Abstract: The present invention relates to novel substituted pyrrole compounds, their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them. This invention particularly relates to novel substituted pyrrole compounds of the general formula (I), their analogs, their derivatives, their polymorphs, their tautomeric forms, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and their pharmaceutical compositions containing them.
    Type: Application
    Filed: August 10, 2001
    Publication date: October 23, 2003
    Applicant: CADILA HEALTHCARE LIMITED
    Inventors: Braj Bhushan Lohray, Vidya Bhushan Lohray, Vijay Kumar Gajubhai Barot
  • Patent number: 6603012
    Abstract: New compounds containing bicyclic fused rings, one of which being a phenyl moiety connected by an aliphatic chain to a cycloalkyl or aryl moiety, and pharmaceutically active salts thereof are useful as RAR selective retinoid agonists. Furthermore, such retinoic acid receptor agonists, particularly retinoic acid receptor &ggr; (RAR&ggr;) selective agonists, are useful for the treatment of emphysema and associated pulmonary diseases, as well as for the therapy and prophylaxis of dermatological disorders, for the therapy and prophylaxis of malignant and premalignant epithelial lesions, tumors and precancerous changes of the mucous membrane in the mouth, tongue, larynx, esophagus, bladder, cervix and colon.
    Type: Grant
    Filed: April 23, 2001
    Date of Patent: August 5, 2003
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Paula Nanette Belloni, Synese Jolidon, Michael Klaus, Jean-Marc Lapierre
  • Patent number: 6593345
    Abstract: The instant invention provides novel substituted naphthyl compounds, intermediates, compositions, pharmaceutical formulations, and methods of use.
    Type: Grant
    Filed: August 27, 1997
    Date of Patent: July 15, 2003
    Assignee: Eli Lilly and Company
    Inventors: Henry Uhlman Bryant, Thomas Alan Crowell, Charles David Jones, Alan David Palkowitz
  • Patent number: 6576780
    Abstract: The current invention discloses hydroxyamidino derivatives useful as nitric oxide synthase inhibitors.
    Type: Grant
    Filed: October 13, 2000
    Date of Patent: June 10, 2003
    Assignee: GD Searle & Company
    Inventors: Rolando E. Gapud, Timothy J. Hagen, E. Ann Hallinan, Donald W. Hansen, Jr., Barnett S. Pitzele, Suzanne S. Metz, R. Keith Webber, Foe S. Tjoeng, Robert E. Manning, Mihaly V. Toth
  • Patent number: 6559100
    Abstract: Substituted 2-benzoylcyclohexane-1,3-diones of the formula I where: R1 and R2 are each hydrogen, mercapto, nitro, halogen, cyano, thiocyanato, C1-C6-alkyl, C1-C6-haloalkyl, C1-C6-alkoxy, C2-C6-alkenyl, C2-C6-alkynyl, —OR3, —OCOR3, —OSO2R3, —S(O)nR3, —SO2OR3, —SO2N(R3)2, —NR3SO2R3 or —NR3COR3; R3 is hydrogen, C1-C6-alkyl, C1-C6-haloalkyl, C2-C6-alkenyl, C2-C6-alkynyl, phenyl or phenyl-C1-C6-alkyl; where the abovementioned alkyl radicals may be partially or fully halogenated and/or may carry one to three of the following groups: hydroxyl, mercapto, amino, cyano, R3, —OR3, —SR3, —N(R3)2, ═NOR3, —OCOR3, —SCOR3, —NR3COR3, —CO2R3, —COSR3, —CON(R3)2, C1-C4-alkyliminooxy, C1-C4-alkoxyamino, C1-C4-alkylcarbonyl, C1-C4-alkoxy-C2-C6-alkoxycarbonyl, C1-C4-alkylsulfonyl, heterocyclyl, heterocyclyloxy, phenyl, benzyl, hetaryl, phenoxy, benzyloxy and hetaryloxy, where the eight last mentioned radic
    Type: Grant
    Filed: February 7, 2000
    Date of Patent: May 6, 2003
    Assignee: BASF Aktiengesellschaft
    Inventors: Stefan Engel, Joachim Rheinheimer, Ernst Baumann, Wolfgang von Deyn, Regina Luise Hill, Guido Mayer, Ulf Misslitz, Oliver Wagner, Matthias Witschel, Martina Otten, Helmut Walter, Karl-Otto Westphalen
  • Patent number: 6541506
    Abstract: The invention features enediynes and methods for their production and use. The enediynes of the invention have the formula: wherein R1 is a hydroxyl group or a moiety that can be replaced by a hydroxyl group in a hydrolysis reaction; each R2 is, independently, H or a monovalent hydrocarbon moiety containing between 1 and 4 carbon atoms, inclusive; R3 is a pyrrole, furan, or thiophene ring; and X is an integer between 4 and 10, inclusive.
    Type: Grant
    Filed: October 5, 2000
    Date of Patent: April 1, 2003
    Assignee: Phytera Incorporated
    Inventors: Baoliang Cui, James Bruce McAlpine, Maureen Kelly Talbot, Shu-Wei Yang, Catherine Heintz, Angela Stafford
  • Patent number: 6541475
    Abstract: &agr;, &bgr;-Unsaturated sulfones of the following formulae are provided, which are useful as antiproliferative agents, including, for example, anticancer agents:
    Type: Grant
    Filed: April 12, 2001
    Date of Patent: April 1, 2003
    Assignee: Temple University - Of the Commonwealth System of Higher Education
    Inventors: E. Premkumar Reddy, M. V. Ramana Reddy
  • Patent number: 6518429
    Abstract: The present invention relates to novel imidazole derivatives which show an inhibitory activity against farnesyl transferase, pharmaceutically acceptable salts or isomers thereof and pharmaceutical compositions comprising such imidazole derivatives. More particularly, the present invention relates to intermediate compounds which are used in the preparation of the imidazole derivatives of the invention. Related processes also are disclosed.
    Type: Grant
    Filed: March 20, 2001
    Date of Patent: February 11, 2003
    Assignee: LG Chemical, Ltd.
    Inventors: Hyun Il Lee, Jong Sung Koh, Jin Ho Lee, Won Hee Jung, You Seung Shin, Hyun Ho Chung, Jong Hyun Kim, Seong Gu Ro, Tae Saeng Choi, Shin Wu Jeong, Tae Hwan Kwak, In Ae Ahn, Hyun Sung Kim, Sun Hwa Lee, Kwi Hwa Kim, Jung Kwon Yoo
  • Patent number: 6506863
    Abstract: Esters of 3-(2-furyl)-2-propenoic acid with diols having the general formula A2X, in which A is a 3-(2-furyl)-2-propenoate group and X is a C1-C6 alkylene group. The said esters are used as crosslinking agents in processes for crosslinking polymers.
    Type: Grant
    Filed: December 14, 2001
    Date of Patent: January 14, 2003
    Assignee: Basell Poliolefine Italia S.p.A.
    Inventors: Francesco Romani, Vittorio Braga
  • Publication number: 20030008996
    Abstract: A radical polymerizable compound comprising a structure represented by the following formula (I), (II) or (III): 1
    Type: Application
    Filed: March 14, 2002
    Publication date: January 9, 2003
    Inventor: Kazuto Kunita
  • Patent number: 6482859
    Abstract: The invention relates to novel pesticidally active compounds of the general formula I as well as possible isomers and mixtures of isomers thereof, wherein n is a number zero or one; and R1 is C1-C12alkyl that is unsubstituted or may be substituted by C1-C4alkoxy, C1-C4alkylthio, C1-C4alkylsulfonyl, C3-C8cycloalkyl, cyano, C1C6alkoxycarbonyl, C3-C6alkenyloxycarbonyl or by C3-C6alkynyloxycarbonyl; C3-C8cycloalkyl; C2-C12alkenyl; C2-C12alkynyl; C1-C12haloalkyl: or a group NR11R12 wherein R11 and R12 are each independently of the other hydrogen or C1-C8alkyl, or together are tetra- or penta-methylene; R2 and R3 are each independently of the other hydrogen; C1-C8alkyl; C1-C8alkyl substituted by hydroxy, C1-C4alkoxy, mercapto or by C1-C4alkylthio; C3-C8alkenyl; C3-C8alkynyl; C3-C8cycloalkyl; C3-C8cycloalkyl-C1-C4alkyl; or the two groups R2 and R3 together with the carbon atom to which they are bonded form a three- to eight-membered ring; R4, R5, R6 and R7 are identical or different and are ea
    Type: Grant
    Filed: February 4, 2000
    Date of Patent: November 19, 2002
    Assignee: Syngenta Crop Protection, Inc.
    Inventors: Martin Zeller, André Jeanguenat
  • Patent number: 6458803
    Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-phenyl-N-heteroaralkyl aminoalcohols.
    Type: Grant
    Filed: November 23, 2001
    Date of Patent: October 1, 2002
    Assignee: G.D. Searle & Co.
    Inventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
  • Patent number: 6441177
    Abstract: Tertiary amines of the formula wherein A1, A2, A3, A4, M, p, T and Q are as defined herein, and acid addition salts thereof, have antimycotic and cholesterol-lowering activity.
    Type: Grant
    Filed: December 16, 1999
    Date of Patent: August 27, 2002
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Johannes Aebi, Henrietta Dehmlow, Jacques Himber, Synèse Jolidon, Hans Lengsfeld, Olivier Morand, Gérard Schmid, Yu-Hua Ji
  • Patent number: 6391827
    Abstract: The invention relates to pyrrolic compounds having formula The compounds having formula (I) have a high herbicidal activity and are used for controlling weeds in the agronomic field
    Type: Grant
    Filed: June 15, 2000
    Date of Patent: May 21, 2002
    Assignee: Isagro Ricerca S.r.l.
    Inventors: Giovanni Meazza, Franco Bettarini, Paolo Castoro, Piero La Porta, Ernesto Signorini, Domenico Portoso
  • Patent number: 6376681
    Abstract: This invention relates to the drug, ketorolac and the synthesis of compounds useful in the manufacture of ketorolac. Ketorolac tromethamine is a pharmaceutical compound useful as an analgesic.
    Type: Grant
    Filed: December 6, 2000
    Date of Patent: April 23, 2002
    Assignee: Mallinckodt Inc.
    Inventors: John R. Duchek, Henry J. Buehler, Douglas C. Caskey
  • Patent number: 6358995
    Abstract: The present invention provides a medicament exhibiting excellent retinoic acid receptor agonism. A Carboxylic acid derivative having a fused ring which is represented by the following formula or a pharmacologically acceptable salt thereof: {wherein the symbol represents a single bond or a double bond; X, Y, Z, P, Q, U, V and W are each a group represented by the formula: —O— or —S—, or a group represented by the formula: [wherein Rk (k: 1 to 8) is hydrogen, halogeno, optionally substituted lower alkyl or the like, with either of R7 and R8 being a group represented by the formula: (wherein A and B are each independently an optionally substituted aromatic hydrocarbon ring or an optionally substituted unsaturated heterocycle; and D is optionally protected carboxyl)]}.
    Type: Grant
    Filed: July 21, 2000
    Date of Patent: March 19, 2002
    Assignee: Eisai Co., Ltd.
    Inventors: Katsuya Tagami, Hiroyuki Yoshimura, Mitsuo Nagai, Shigeki Hibi, Kouichi Kikuchi, Takashi Sato, Makoto Okita, Yasushi Okamoto, Yumiko Nagasaka, Naoki Kobayashi, Takayuki Hida, Kenji Tai, Naoki Tokuhara, Seiichi Kobayashi
  • Patent number: 6355810
    Abstract: Disclosed are multibinding compounds which inhibit 3-hydroxy-3-methylglutaryl coenzyme A reductase (HMG-COA reductase), the rate limiting enzyme in cholesterol biosynthesis. The multibinding compounds of this invention containing from 2 to 10 ligands covalently attached to one or more linkers. Each ligand is a moiety capable of binding to HMG-CoA reductase and the distance between ligands is at least 10 Å. The multibinding compounds of this invention are useful in the treatment and prevention of hypercholesterolemia, hyperlipidemia, atherosclerosis and the like.
    Type: Grant
    Filed: June 4, 1999
    Date of Patent: March 12, 2002
    Assignee: Advanced Medicine, Inc.
    Inventors: John H. Griffin, Michael R. Leadbetter, Donald E. Schmidt, Jr.
  • Patent number: 6331636
    Abstract: This invention is therapeutically useful 2-aminotetralins and pharmaceutically acceptable acid addition salts thereof of the formula These compounds are useful to treat central nervous system disorders, hypertension, diabetes, sexual impotency and to control appetite.
    Type: Grant
    Filed: March 12, 1992
    Date of Patent: December 18, 2001
    Assignee: The Upjohn Company
    Inventors: Arthur G. Romero, William H. Darlington
  • Patent number: 6323202
    Abstract: The invention provides compounds of the formula 1 that are active against the HSV primase enzyme: wherein R1 is hydroxy or amino; R2 is hydrogen, halo, (C1-4)alkyl or (C1-4)alkoxy; R3 is hydrogen, halo, (C1-4)alkyl, (C1-4)alkoxy, amino or azido; R4 has the same significance as R2; R5 is hydrogen or (C1-4)alkyl; and R is (C1-7)alkyl, (C3-6)cycloalkyl, {phenyl(C1-7)alkyl}, {phenyl(C1-7)alkoxy}, {{(monocyclic heterocyclo)-{(C1-7)alkoxy}}, CH(W)C(O){O-(C1-4)alkyl} wherein W is hydrogen or (C1-7)alkyl, or  wherein Y is hydrogen or (C1-7)alkyl, and Z is (C1-7)alkyl, (C3-6) cycloalkyl, {(C3-6)cycloalkyl}- {(C1-7)alkyl}, phenyl(C1-7)alkyl or {{(monocyclic heterocyclo)-{(C1-7)alkyl}}, or Y and Z together with the nitrogen atom to which they are attached represent, 1-pyrrolidinyl, 1-piperidinyl, 4-morpholinyl or 1-(4-methylpiperazinyl); with the provisos that (1) when R is CH(W
    Type: Grant
    Filed: March 24, 2000
    Date of Patent: November 27, 2001
    Assignee: Boehringer Ingelheim (Canada) Ltd.
    Inventors: Bruno Simoneau, Michele Liuzzi, Anton Mentrup
  • Patent number: 6320059
    Abstract: There is provided a process for the preparation of 2-aryl-5-(perfluoroalkyl)pyrrole compounds from N-[1-chloro-1-(perfluoroalkyl)methyl]arylimidoyl chloride compounds. The 2-aryl-5-(perfluoroalkyl)pyrrole compounds are useful for the control of insect and acrid pests, and may also be used to prepare other pesticidal arylpyrrole compounds. In addition, the present invention provides compounds which are useful as intermediates in the preparation of arylpyrrole compounds.
    Type: Grant
    Filed: March 7, 2000
    Date of Patent: November 20, 2001
    Assignee: American Cyanamid Company
    Inventor: Venkataraman Kameswaran
  • Patent number: 6310217
    Abstract: The invention provides novel antiinflammatory and analgesic agents of the formulae The novel compounds have an improved inhibitory effect and/or less cytotoxicity in comparison with compounds known from the prior art. The compounds according to the invention are outstandingly suitable for preventing and/or treating disorders caused or partly caused by an increased activity of the enzyme phospholipase A2, such as, for example, inflammations, allergies, asthma, psoriasis and endotoxic shock.
    Type: Grant
    Filed: January 29, 1999
    Date of Patent: October 30, 2001
    Assignee: Merckle GmbH
    Inventor: Matthias Lehr
  • Patent number: 6294568
    Abstract: The present invention provides compounds represented by the general formula (I): and a salt thereof, and anti-inflammatory agents and antitumor agents containing the compounds as the active ingredients.
    Type: Grant
    Filed: June 26, 2000
    Date of Patent: September 25, 2001
    Assignee: Nissin Food Products Co., Ltd.
    Inventors: Toshihiro Yamada, Yoichi Nobuhara, Kazuhiro Kobayashi, Satoshi Hirano, Takanobu Sakurai, Hiroshi Mikami, Ayako Miyake
  • Patent number: 6288241
    Abstract: A new crystalline form of 1-methyl-5-p-toluoylpyrrole-2-acetamidoacetic acid guaiacyl ester, a process for its preparation and pharmaceutical compositions endowed of anti-inflammatory, analgesic and antipyretic activity containing same are disclosed.
    Type: Grant
    Filed: June 12, 2000
    Date of Patent: September 11, 2001
    Assignee: Sigma-Tau Farmaceutiche Riunite S.p.A.
    Inventor: Sergio Anzalone
  • Patent number: 6277849
    Abstract: The invention relates to novel pesticidally active compounds of the general formula I as well as possible isomers and isomeric mixtures thereof, wherein n is a number zero or one; and R1 is C1-C12alkyl that is unsubstituted or may be substituted by C1-C4alkoxy, C1-C4alkylthio, C1-C4alkylsulfonyl, C3-C8acycloalkyl, cyano, C1-C6alkoxycarbonyl, C3-C8alkenyloxycarbonyl, C1-C5alkynyloxycarbonyl; C3-C8cycloalkyl; C2-C12alkenyl: C2-C12alknyl; C1-C12haloalkyl or a group NR11R12; wherein R11, and R12 are each independently of the other hydrogen, C1-C6alkyl or together are tetra- or penta-methylene; R2 and R3 are each independently of the other hydrogen; C1-C8alkyl; C1-C8alkyl substituted by hydroxy, C1-C4alkoxy, mercapto or by C1C4alkylthio; C3-C8alkenyl; C3-C8alkynyl; C3-C8cycloalkyl; C3-C8acycloalkyl-C1-C4alkyl or wherein the two groups R2 and R3 together with the carbon atom to which they are bonded form a three- to eight-membered ring; R4, R5, R6 and R7 are identical or different and are eac
    Type: Grant
    Filed: August 24, 1999
    Date of Patent: August 21, 2001
    Assignee: Syngenta Crop Protection, Inc.
    Inventor: Martin Zeller
  • Patent number: 6277833
    Abstract: Substituted triols are prepared by reducing appropriately substituted carboxylic esters. The substituted triols can be used as active substances in medicaments.
    Type: Grant
    Filed: September 24, 1998
    Date of Patent: August 21, 2001
    Assignee: Bayer Aktiengesellschaft
    Inventors: Rolf Angerbauer, Peter Fey, Walter Hübsch, Thomas Philipps, Hilmar Bischoff, Hans-Peter Krause, Jörg Petersen von Gehr, Delf Schmidt
  • Patent number: 6248765
    Abstract: Novel imidazole derivatives as histamine receptor H3 antagonists and/or agonists, preparation thereof and therapeutical uses thereof. Chemical compounds for use as histamine receptor H3 agonists, partial agonists or antagonists, having general formula (Ia) or (Ib), the use thereof for making drugs, and methods for revealing the agonist, partial agonist or antagonist activity of such compounds in vivo, are disclosed.
    Type: Grant
    Filed: January 9, 1997
    Date of Patent: June 19, 2001
    Assignees: Institut National de la Sante et de la Recherche Medical, Societe Civile Bioprojet
    Inventors: Jean-Charles Schwartz, Jean-Michel Arrang, Monique Garbarg, Agnes Quemener, Jeanne-Marie Lecomte, Xavier Ligneau, Walter G. Schunack, Holger Stark, Katja Purand, Annette Huls, Reidemeister Sybille, Athmani Salah, Charon Robbin Ganellin, Nadia Pelloux-Leon, Wasyl Tertiux, Michael C. O. Krause, Sadek Bassem
  • Patent number: 6242613
    Abstract: The present invention relates to arylpyrrole particles which are prepared by a process in which the particles are aged and milled, and pesticidal suspension concentrate compositions comprising them. The size of the particles of this invention remains surprisingly stable during storage.
    Type: Grant
    Filed: April 6, 1999
    Date of Patent: June 5, 2001
    Assignee: American Cyanamid Co.
    Inventors: Mimi Yih-Pei Chou Schaaf, Steven Brunt, Jian James Xu, Andrew Evelyn Goldsmith, Anthony Francis Walker, Patrick C. Mowery, Edward S. Donoghue, Srinivasan Rajan
  • Patent number: 6222064
    Abstract: A fluorination method of oxygen and halogen sites with diaryl-, dialkoxyalkyl-, alkylalkoxyalkyl-, arylalkoxyalkyl- and cyclic aminosulfur trifluorides fluorinating reagents is disclosed.
    Type: Grant
    Filed: January 14, 2000
    Date of Patent: April 24, 2001
    Assignee: Air Products and Chemicals, Inc.
    Inventors: Gauri Sankar Lal, Guido Peter Pez
  • Patent number: RE39420
    Abstract: Compounds of formula (I) and (II): [wherein R is hydrogen, halogen or alkyl; R1 is alkyl, amino or substituted amino; R2 is optionally substituted phenyl; R3 is hydrogen, halogen or optionally substituted alkyl; R4 is hydrogen, optionally substituted alkyl, cycloalkyl, aryl, or aralkyl] have valuable analgesic, anti-inflammatory, anti-pyretic and anti-allergic activities and have the ability to inhibit the production of leukotrienes and to inhibit bone resorption. They are relatively free from the side effects which generally result from the administration of compounds having these kinds of activities.
    Type: Grant
    Filed: September 29, 2000
    Date of Patent: December 5, 2006
    Assignee: Sankyo Company, Limited
    Inventors: Tomio Kimura, Yasuo Noguchi, Akira Nakao, Keisuke Suzuki, Shigeru Ushiyama, Akihiro Kawara, Masaaki Miyamoto