The Additional Hetero Ring Is Bonded Directly To A Ring Carbon Of The Bicyclo Ring System Patents (Class 548/466)
  • Publication number: 20080234494
    Abstract: A compound of formula I wherein R, Ra, Rb, Rc, Rd and Re are as defined in the specification, processes for their production, their uses, in particular in transplantation, and pharmaceutical compositions containing them.
    Type: Application
    Filed: January 19, 2005
    Publication date: September 25, 2008
    Inventors: Maurice Van Eis, Peter Von Matt, Jurgen Wagner, Jean-Pierre Evenou
  • Publication number: 20080227842
    Abstract: The invention relates to a compound of formula (I), or a pharmacologically or cosmetically acceptable salt or derivative thereof, wherein R1 to R5 are selected from the groups R1 representing -alkyl, -vinyl, —CHOH—CH2OH, R2 representing H, —OH, —Oalkyl, —Oacyl, saccharide groups, modified saccharide groups (e.g. malonylated), R3 representing —H, —OH, —Oalkyl, —Oacyl, modified —Oacyl (e.g. malonylated), saccharide groups, modified saccharide groups (e.g. malonylated), R4, R5 representing —COOH, -carbonic esters, for use as drug, antioxidant, food supplement. The invention also relates to a method for producing the compound of formula (I).
    Type: Application
    Filed: March 11, 2008
    Publication date: September 18, 2008
    Inventors: Bernhard Krautler, Thomas Muller
  • Patent number: 7425553
    Abstract: The present invention relates to novel Triheterocyclic Compounds, compositions comprising a Triheterocyclic Compound, and methods useful for treating or preventing cancer or a neoplastic disorder comprising administering a Triheterocyclic Compound. The compounds, compositions, and methods of the invention are also useful for inhibiting the growth of a cancer cell or neoplastic cell, treating or preventing a viral infection, or inhibiting the replication and/or infectivity of a virus.
    Type: Grant
    Filed: May 28, 2004
    Date of Patent: September 16, 2008
    Assignee: Gemin X Pharmaceuticals Canada inc.
    Inventors: Giorgio Attardo, Jean-Francois Lavallee, Elise Rioux, Terrence W. Doyle
  • Publication number: 20080221160
    Abstract: Compounds of the following structure are provided, wherein n, R1-R3 and R6-R9 are defined below, as are methods of preparing and using these compounds for contraception; treating or preventing fibroids, uterine leiomyomata, endometriosis, dysfunctional bleeding, polycystic ovary syndrome, and hormone-dependent carcinomas; providing hormone replacement therapy; stimulating food intake; synchronizing estrus; and treating cycle-related symptoms.
    Type: Application
    Filed: March 4, 2008
    Publication date: September 11, 2008
    Applicant: Wyeth
    Inventors: Casey Cameron McComas, Andrew Fensome
  • Patent number: 7405300
    Abstract: The present invention relates to a series of substituted indole derivatives of the formula I: wherein R, R1, R2, R3, R4, X and Y are as defined herein. This invention also relates to methods of making these compounds. The compounds of this invention are inhibitors of poly(adenosine 5?-diphosphate ribose) polymerase (PARP) and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases, including diseases associated with the central nervous system and cardiovascular disorders.
    Type: Grant
    Filed: September 1, 2004
    Date of Patent: July 29, 2008
    Assignee: Aventis Pharmaveuticals Inc.
    Inventors: John Z. Jiang, Jack Roger Koehl, Shujaath Mehdi, Neil David Moorcroft, Kwon Yon Musick, Philip Marvin Weintraub, Paul Robert Eastwood
  • Publication number: 20080146587
    Abstract: Compounds of formula I or formula II: or pharmaceutically acceptable salts thereof, wherein m, n, p, Ar R1, R2, R4, and R5 are as defined herein. The invention also provides methods for preparing, compositions comprising, and methods for using compounds.
    Type: Application
    Filed: November 8, 2007
    Publication date: June 19, 2008
    Inventors: Joe Timothy Bamberg, Counde O'Yang, Meng Sui, Shu-Hai Zhao
  • Publication number: 20080119490
    Abstract: An isomer, enantiomer, diastereoisomer or tautomer of a compound, represented by formula I: wherein A, B, R2, R3, M1, M2, M3, M4, Y1 and Z are as defined in claim 1, or a salt thereof, as an inhibitor of HCV NS5B polymerase.
    Type: Application
    Filed: November 30, 2007
    Publication date: May 22, 2008
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Marc-Andre POUPART, Pierre Louis BEAULIEU, Jean RANCOURT
  • Patent number: 7375219
    Abstract: The present invention features inhibitors of nitric oxide synthase (NOS), particularly those that selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms. The NOS inhibitors of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing conditions such as, for example, stroke, reperfusion injury, neurodegeneration, head trauma, CABG, migraine headache with and without aura, migraine with allodynia, central post-stroke pain (CPSP), neuropathic pain, morphine/opioid induced tolerance and hyperalgesia.
    Type: Grant
    Filed: April 13, 2006
    Date of Patent: May 20, 2008
    Assignee: NeurAxon, Inc.
    Inventors: Shawn Maddaford, Jailall Ramnauth, Suman Rakhit, Joanne Patman, Paul Renton, Subhash C. Annedi
  • Patent number: 7371868
    Abstract: Process for producing a 7-bromoquinolone-carboxylic acid derivative of the following formula or its salt by reacting a 2,4-dibromo-3-hydroxybenzoic acid ester compound of the formula R7a-x to obtain a 3-alkoxy-2,4-dibromobenzoic acid ester, subjecting the 3-alkoxy-2,4-dibromobenzoic acid ester to elimination reaction of the carboxyl-protecting group to obtain a 3-alkoxy-2,4-dibromobenzoic acid, subjecting the 3-alkoxy-2,4-dibromobenzoic acid to ketoesterification reaction to obtain a 3-alkoxy-2,4-dibromobenyolacetic acid ester, reacting the 3-alkoxy-2,4-dibromobenzoylacetic acid ester with an orthoester or an acetal, then reacting the reaction product with a compound of the formula R2—NH or its salt to obtain a 2-(3-alkoxy-2,4-dibromobenzoyl)-3-substituted aminoacrylic acid ester and subjecting the 2-(3-alkoxy-2,4-dibromobenzoyl)-3-substituted aminoacrylic acid ester to ring-closing reaction, and products thereof.
    Type: Grant
    Filed: March 27, 2007
    Date of Patent: May 13, 2008
    Assignee: Toyama Chemical Co., Ltd.
    Inventors: Katsuji Ojima, Tamotsu Takamatsu, Kyoko Taya, Taro Kiyoto
  • Publication number: 20080045560
    Abstract: Compounds of the following structure are described: wherein R1-R6, R11, R12, m, V, X, Y, Z and Q are described herein, or a pharmaceutically acceptable salt, tautomer, metabolite or prodrug thereof. These compounds are useful for treating a variety of hormone-related conditions including contraception, treating or preventing fibroids, endometriosis, dysfunctional bleeding, uterine leiomyomata, polycystic ovary syndrome, or hormone-dependent carcinomas, providing hormone replacement therapy, stimulating food intake or synchronizing estrus.
    Type: Application
    Filed: August 13, 2007
    Publication date: February 21, 2008
    Applicant: Wyeth
    Inventors: Thomas Joseph Commons, Andrew Fensome, Gavin David Heffernan, Casey Cameron McComas, Richard Page Woodworth, Michael Byron Webb, Michael Anthony Marella, Edward George Melenski
  • Publication number: 20080027122
    Abstract: Novel indole derivatives of formula (I) or a pharmaceutically acceptable salt thereof: wherein R1 is fluorine, or chlorine, and R2 is hydrogen, or fluorine, which are SGLT inhibitors and are useful for treatment or prevention of diabetes and related conditions.
    Type: Application
    Filed: July 26, 2007
    Publication date: January 31, 2008
    Inventors: Sumihiro Nomura, Shigeki Sakamaki
  • Patent number: 7323470
    Abstract: An isomer, enantiomer, diastereoisomer or tautomer of a compound, represented by formula I: wherein wherein A, B, R2, R3, M1, M2, M3, M4, Y1 and Z are as defined in claim 1, or a salt thereof, as an inhibitor of HCV NS5B polymerase.
    Type: Grant
    Filed: April 17, 2006
    Date of Patent: January 29, 2008
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Marc-André Poupart, Pierre Louis Beaulieu, Jean Rancourt
  • Patent number: 7317037
    Abstract: Pyrrole-oxindole derivatives useful as progesterone receptor antagonists, and methods for preparing the same, are provided. Pharmaceutical compositions containing these derivatives are described, as is the use thereof in contraception and hormone-related conditions.
    Type: Grant
    Filed: July 6, 2005
    Date of Patent: January 8, 2008
    Assignee: Wyeth
    Inventors: Andrew Fensome, Casey Cameron McComas, Edward George Melenski, Michael Anthony Marella, Jay Edward Wrobel, Gary Sondermann Grubb
  • Publication number: 20070244125
    Abstract: The present invention relates to compounds of formula I wherein G and R1 to R5 and R12 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.
    Type: Application
    Filed: April 5, 2007
    Publication date: October 18, 2007
    Inventors: Matthias Nettekoven, Jean-Marc Plancher, Hans Richter, Olivier Roche, Sven Taylor
  • Patent number: 7282507
    Abstract: The present invention is directed to novel indole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.
    Type: Grant
    Filed: April 1, 2005
    Date of Patent: October 16, 2007
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: James C. Lanter, Zhihua Sui, James J. Fiordeliso, Weiqin Jiang, Xuqing Zhang
  • Patent number: 7271192
    Abstract: Novel 2-pyrrolidin-2-yl-1H-indole compounds corresponding to formula (I) wherein R1, R2, R3 and R4 have the meanings given in the description, and pharmaceutical compositions containing these compounds, as well as processes for the preparation of such compounds and intermediate products of this process, and related methods of treatment.
    Type: Grant
    Filed: June 7, 2004
    Date of Patent: September 18, 2007
    Assignee: Gruenenthal GmbH
    Inventors: Corinna Sundermann, Bernd Sundermann, Helmut Buschmann, Hagen-Heinrich Hennies
  • Patent number: 7265148
    Abstract: The present invention relates generally to substituted pyrrole-indoles such as substituted pyrrole-indoles, and methods of using them.
    Type: Grant
    Filed: September 23, 2004
    Date of Patent: September 4, 2007
    Assignee: Wyeth
    Inventor: Baihua Hu
  • Patent number: 7253203
    Abstract: This invention relates to substituted indoline derivative compounds which are antagonists of the progesterone receptor, their preparation and pharmaceutical utility, particularly including contraception and treatment of benign or malignant neoplastic diseases, having the general structure: wherein R1 and R2 may be single substituents or fused to form spirocyclic rings.
    Type: Grant
    Filed: March 17, 2006
    Date of Patent: August 7, 2007
    Assignee: Wyeth
    Inventors: Andrew Fensome, Lori L. Miller, John W. Ullrich, Reinhold H. W. Bender, Puwen Zhang, Jay E. Wrobel, Lin Zhi, Todd K. Jones, James P. Edwards, Christopher M. Tegley
  • Patent number: 7220774
    Abstract: Indolylmaleimide derivatives comprising either a substituted phenyl, naphthyl, tetrahydronaphthyl, quinazolinyl, quinolyl, isoquinolyl or pyrimidinyl residue have interesting pharmaceutical properties, e.g. in the treatment and/or prevention of T-cell mediated acute or chronic inflammatory diseases or disorders, autoimmune diseases, graft rejection or cancer.
    Type: Grant
    Filed: September 11, 2003
    Date of Patent: May 22, 2007
    Assignee: Novartis AG
    Inventors: Rainer Albert, Claus Ehrhardt, Jean-Pierre Evenou, Richard Sedrani, Peter Von Matt, Jurgen Wagner, Gerhard Zenke
  • Patent number: 7202267
    Abstract: The invention relates to acyloxypyrrolidine derivatives of general formula (I): in which: R1 represents a hydrogen atom, a (C1–C6)alkyl, a (C3–C6)cycloalkyl, a group —CH2CH2COOH or a group —NR2R3; R2 and R3 each represent, independently, a hydrogen atom or a (C1–C6)alkyl. Also disclosed and claimed are the method of preparation of the compounds of the invention and their application in therapeutics.
    Type: Grant
    Filed: January 19, 2005
    Date of Patent: April 10, 2007
    Assignee: Sanofi-aventis
    Inventors: Alain Aulombard, Georges Garcia, Antoine Pradines, Claudine Serradeil-Le Gal, Jean Wagnon
  • Patent number: 7202266
    Abstract: Compounds are described that are active on PPARs, including pan-active compounds. Also described are methods for developing or identifying compounds having a desired selectivity profile.
    Type: Grant
    Filed: July 16, 2004
    Date of Patent: April 10, 2007
    Assignee: Plexxikon, Inc.
    Inventors: James Arnold, Dean R. Artis, Clarence R. Hurt, Prabha N. Ibrahim, Heike Krupka, Jack Lin, Michael V. Milburn, Weiru Wang, Chao Zhang
  • Patent number: 7176200
    Abstract: The present invention relates to new derivatives of sulphonamides, with the general formula (I), as well as to their physiologically acceptable salts, the processes for their preparation, their application as medicaments in human and/or veterinary therapy and the pharmaceutical compositions that contain them
    Type: Grant
    Filed: September 3, 2004
    Date of Patent: February 13, 2007
    Assignee: Laboratories Del Dr. Esteve, S.A.
    Inventors: Ramón Merce-Vidal, Blas Andaluz-Mataro, Jordi Frigola-Constansa
  • Patent number: 7148240
    Abstract: The invention relates to benzofuran or benzothiophene derivatives of general formula: These compounds are of use as medicinal products, in particular in the treatment of pathological syndromes of the cardiovascular system.
    Type: Grant
    Filed: August 23, 2001
    Date of Patent: December 12, 2006
    Assignee: Sanofi-Aventis
    Inventors: Jean-Louis Assens, Claude Bernhart, Frédérique Cabanel-Haudricourt, Dino Nisato
  • Patent number: 7144912
    Abstract: The present invention relates to novel Pyrrole-Type compounds, compositions comprising Pyrrole-Type compounds, and methods useful for treating or preventing cancer or a neoplastic disorder comprising administering a Pyrrole-Type compound. The compounds, compositions, and methods of the invention are also useful for inhibiting the growth of a cancer cell or neoplastic cell. The present invention also relates to novel Pyrrole-Type compounds, compositions, and methods useful for treating or preventing a viral infection. The compounds, compositions, and methods of the invention are also useful for inhibiting the replication and/or infectivity of a virus. The present invention also relates to novel Pyrrole-Type compounds, compositions, and methods useful for causing immunosuppression. The present invention also relates to novel Pyrrole-Type compounds, compositions, and methods useful for treating or preventing an autoimmune disease.
    Type: Grant
    Filed: July 18, 2002
    Date of Patent: December 5, 2006
    Assignee: Gemin X Biotechnologies Inc.
    Inventors: Roy A. Johnson, Giorgio Attardo
  • Patent number: 7129240
    Abstract: The invention relates to compounds of formula: as well as the possible salts thereof with mineral or organic acids, and the solvates and/or hydrates thereof, which have affinity for and selectivity towards the V1b receptors or towards both the V1b and V1a receptors of arginine-vasopressin. The invention also relates to the process for preparing them, to the intermediate compounds of formula (II) that are useful for preparing them, to pharmaceutical compositions containing them and to their use for the preparation of medicinal products.
    Type: Grant
    Filed: April 29, 2004
    Date of Patent: October 31, 2006
    Assignee: Sanofi-Aventis
    Inventors: Richard Roux, Claudine Serradeil-le Gal, Bernard Tonnerre, Jean Wagnon
  • Patent number: 7098231
    Abstract: An isomer, enantiomer, diastereoisomer or tautomer of a compound, represented by formula I: wherein A, B, R2, R3, M1, M2, M3, M4, Y1 and Z are as defined in claim 1, or a salt thereof, as an inhibitor of HCV NS5B polymerase
    Type: Grant
    Filed: January 12, 2004
    Date of Patent: August 29, 2006
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Marc-Andre Poupart, Pierre Louis Beaulieu, Jean Rancourt
  • Patent number: 7094800
    Abstract: The invention relates to compounds of the formula I in which the radicals have the meanings stated in the text, their stereoisomeric forms, and their physiologically tolerated salts, physiologically functional derivatives and process for their preparation. The compounds are suitable for the treatment of disorders of metabolism, such as type 2 diabetes.
    Type: Grant
    Filed: July 26, 2004
    Date of Patent: August 22, 2006
    Assignee: Sanofi-Aventis Deutschland GmbH
    Inventors: Karl Schoenafinger, Holger Wagner, Gerhard Jaehne, Holger Gaul, Christian Buning, Georg Tschank, Ulrich Werner
  • Patent number: 7087750
    Abstract: The invention provides 2, 3-, 4- or 5-substituted-N1-(arylsulfonyl)indole and (heteroaryl)indole compounds of the general formula (I): in which Ar, R2, R3, R4 and R5 are as defined in the specification. The compounds bind to the 5-HT6 receptor and are useful for the treatment and prophylaxis of disorders mediated by the 5-HT6 receptor, such as obesity and CNS disorders.
    Type: Grant
    Filed: October 22, 2001
    Date of Patent: August 8, 2006
    Assignee: Biovitrum AB
    Inventors: Patrizia Caldirola, Björn M. Nilsson, Gary Johansson
  • Patent number: 7056932
    Abstract: The invention is concerned with novel heterocyclyl substituted 1-alkoxy acetic acid derivatives of formula (I) wherein R1 to R6 and A are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit the formation of coagulation factors Xa, IXa and thrombin induced by factor VIIa and tissue factor and can be used as medicaments.
    Type: Grant
    Filed: December 10, 2004
    Date of Patent: June 6, 2006
    Assignee: Hoffman-La Roche Inc.
    Inventors: Luca Claudio Gobbi, Katrin Groebke Zbinden, Peter Mohr, Ulrike Obst
  • Patent number: 7012088
    Abstract: The present invention provides antibacterial agents of formula I described herein and intermediates for their preparation.
    Type: Grant
    Filed: January 22, 2004
    Date of Patent: March 14, 2006
    Assignee: Pharmacia & Upjohn Company
    Inventor: Toni-Jo Poel
  • Patent number: 6900322
    Abstract: A method for stereochemically controlled production of azacyclic compounds of general formula (I) in which the substituents have the meanings given in the specification. The invention also relates to intermediate products of this method and to novel azacyclenes.
    Type: Grant
    Filed: May 10, 1999
    Date of Patent: May 31, 2005
    Assignee: Solvay Pharmaceuticals GmbH
    Inventors: Michael Reggelin, Timo Heinrich, Bernd Junker, Jochen Antel, Ulf Preuschoff
  • Patent number: 6875770
    Abstract: There is provided a compound represented by the general formula (1): wherein Het represents an optional substituted heterocylic group A1 and A2 each independently represent —CH?, etc.; A3 represents —CH2—, etc.; R1 represents a 4-fluorophenyl group, etc.; R2 represents an alkyl group; n represents 0, 1 or 2, provided that when A1 and A2 both are —CH?, A3 represents —CH2— or —SO2—, which is an indole derivative or a mono- or diazaindole derivative that has COX-2 inhibitory activity and is useful as a pharmaceutical, such as an anti-inflammatory agent, or addition salts thereof with a pharmaceutically acceptable acid or base, or hydrates thereof.
    Type: Grant
    Filed: October 1, 2003
    Date of Patent: April 5, 2005
    Assignee: Chugai Seiyaku Kabushiki Kaisha
    Inventors: Hiroharu Matsuoka, Nobuaki Kato, Tadakatsu Takahashi, Noriaki Maruyama, Takenori Ishizawa, Yukio Suzuki
  • Patent number: 6787651
    Abstract: Disclosed are substituted indoles, pharmaceutical compositions containing such indoles, and their use in treating or preventing PPAR-&ggr; mediated diseases or conditions, such as osteopenia, osteoporosis, cancer, diabetes and atherosclerosis.
    Type: Grant
    Filed: October 9, 2001
    Date of Patent: September 7, 2004
    Assignee: SmithKline Beecham Corporation
    Inventors: Andreas Stolle, Jacques P. Dumas, William Carley, Philip D. G. Coish, Steven R. Magnuson, Yamin Wang, Dhanapalan Nagarathnam, Derek B. Lowe, Ning Su, William H. Bullock, Ann-Marie Campbell, Ning Qi, Jeremy L. Baryza, James H. Cook
  • Patent number: 6767912
    Abstract: The present invention provides a compound of formula I and the use thereof in the therapeutic treatment of disorders related to or affected by the 5-HT6 receptor.
    Type: Grant
    Filed: December 20, 2001
    Date of Patent: July 27, 2004
    Assignee: Wyeth
    Inventors: Ping Zhou, Derek Cecil Cole, Michael Gerard Kelly, William Joseph Lennox
  • Patent number: 6750241
    Abstract: Disclosed are compounds which inhibit or modulate the activity of protein kinases and pharmaceutical compositions containing such compounds. The disclosed compound contain two or more ligand moieties covalently linked together by one or more linking groups. Such compounds are useful for treating diseases or medical disorders mediated by protein kinases.
    Type: Grant
    Filed: March 6, 2002
    Date of Patent: June 15, 2004
    Assignee: Theravance, Inc.
    Inventors: John H. Griffin, Yu-Hua Ji, Edmund J. Moran, Jonathan W. Wray
  • Patent number: 6730695
    Abstract: The invention relates to compounds of formula: as well as the possible salts thereof with mineral or organic acids, and the solvates and/or hydrates thereof, which have affinity for and selectivity towards the V1b receptors or towards both the V1b and V1a receptors of arginine-vasopressin. The invention also relates to the process for preparing them, to the intermediate compounds of formula (II) that are useful for preparing them, to pharmaceutical compositions containing them and to their use for the preparation of medicinal products.
    Type: Grant
    Filed: July 24, 2002
    Date of Patent: May 4, 2004
    Assignee: Sanofi-Synthelabo
    Inventors: Richard Roux, Claudine Serradeil-Le Gal, Bernard Tonnerre, Jean Wagnon
  • Patent number: 6699886
    Abstract: The present invention provides store operated calcium influx inhibitor compounds, pharmaceutical compositions, and methods of use. The compounds are useful for treating an inflammatory disease or treating an inflammatory reaction. Preferably, compounds, compositions and methods of this invention are used for treatment of inflammatory skin, pulmonary, musculoskeletal, and gastrointestinal diseases, as well as autoimmune disorders, transplantation treatment, and osteoporosis.
    Type: Grant
    Filed: May 31, 2002
    Date of Patent: March 2, 2004
    Assignee: Cellegy Pharmaceuticals, Inc.
    Inventors: Thomas P. Parks, Don R. Baker
  • Patent number: 6689806
    Abstract: The invention relates to certain indolinone compounds, their method of synthesis, and a combinatorial library consisting of the indolinone compounds of the invention. The invention also relates to methods of modulating the function of protein kinases using indolinone compounds of the invention and methods of treating diseases by modulating the function of protein kinases and related signal transduction pathways.
    Type: Grant
    Filed: March 22, 2000
    Date of Patent: February 10, 2004
    Assignee: Sugen, Inc.
    Inventors: Peng Cho Tang, Li Sun, Gerald McMahon, Todd Anthony Miller, Shahrzad Shirazian, Chung Chen Wei, G. Davis Harris, Jr., Xiaoyuan Li, Congxin Liang
  • Patent number: 6673797
    Abstract: There is provided a compound represented by the general formula (1): wherein Het represents an optionally substituted heterocyclic group; A1 and A2 each independently represent —CH═, etc.; A3 represents —CH2—, etc.; R1 represents a 4-fluorophenyl group, etc.; R2 represents an alkyl group; n represents 0, 1 or 2, provided that when A1 and A2 both are —CH═, A3 represents —CH2— or —SO2—, which is an indole derivative or a mono- or diazaindole derivative that has COX-2 inhibitory activity and is useful as a pharmaceutical, such as an anti-inflammatory agent, or addition salts thereof with a pharmaceutically acceptable acid or base, or hydrates thereof.
    Type: Grant
    Filed: November 27, 2000
    Date of Patent: January 6, 2004
    Assignee: Chugai Seiyaku Kabushiki Kaisha
    Inventors: Hiroharu Matsuoka, Nobuaki Kato, Tadakatsu Takahashi, Noriaki Maruyama, Takenori Ishizawa, Yukio Suzuki
  • Patent number: 6630463
    Abstract: Described is a heterocycle-containing carboxylic acid derivative represented by the following formula (I): wherein A represents, for example, a heteroaryl group which contains at least one nitrogen atom and may have a substituent, B represents, for example, a heteroarylene group, a —CONH— group or a group represented by the formula —CR6═CR7— in which R6 and R7 represents H, a lower alkyl group or the like, D represents an arylene group, a heteroarylene group or the like, n1 stands for 0 or 1, M represents, for example, a hydroxyl group or a lower alkoxy group; or a physiologically acceptable salt thereof. As a retinoic-related compound replacing retinoic acid, it permits the provision of a preventive and/or therapeutic for various diseases.
    Type: Grant
    Filed: July 23, 2001
    Date of Patent: October 7, 2003
    Assignee: Eisai Co. Ltd.
    Inventors: Kouichi Kikuchi, Katsuya Tagami, Hiroyuki Yoshimura, Shigeki Hibi, Mitsuo Nagai, Shinya Abe, Makoto Okita, Takayuki Hida, Seiko Higashi, Naoki Tokuhara, Seiichi Kobayashi
  • Patent number: 6605633
    Abstract: The present invention relates to novel compounds which inhibit the action of CXC chemokines, such as IL-8, Gro, NAP-2, ENA-78 etc., on their receptors, to the process for their preparation and to their use for obtaining drugs. According to the invention, said compounds are novel indole derivatives selected from the group consisting of: i) the products of the formula  in which: X is a double bond —C═C— or a sulfur atom; R1 is a halogen, a nitro group, a trifluoromethyl group or a C1-C3 alkyl group; R2, R3 and R4 are each independently a hydrogen atom, a halogen, a C1-C3 alkyl group, a nitro group, a trifluoromethyl group or a cyano group, or R2 and R3 form a fused aromatic ring together with the aromatic ring to which they are attached; and n is equal to 2 or 3; and ii) esters of the compounds of formula I and addition salts of said compounds with a mineral or organic base.
    Type: Grant
    Filed: May 16, 2002
    Date of Patent: August 12, 2003
    Assignee: Fournier Industrie et Sante
    Inventors: Jean-Luc Paquet, Martine Barth, Didier Pruneau, Pierre Dodey
  • Publication number: 20030121113
    Abstract: Oxobenzofuranylidene-dihydroindolones of formulae trans-(Ia) and cis-(Ib) 1
    Type: Application
    Filed: December 18, 2002
    Publication date: July 3, 2003
    Inventors: Peter Nesvadba, Joachim Jandke
  • Patent number: 6576656
    Abstract: An oxindole of Formula 1 or a prodrug thereof, or a pharmaceutically acceptable salt thereof is useful for growth hormone releaser: wherein R1, R2, R3 and R4 are independently hydrogen, optionally substituted alkyl etc; R5 is optionally substituted aryl or optionally substituted heteroaryl; Z is —O— or —NH—; one of W1 and W2 is hydrogen, alkyl or —Y—CON(R10)R11; the other of W1 and W2 is n is 1, 2 or 3; m is 0, 1, 2 or 3; Y is single bond or C1-C3 alkylene; R6 and R7 are independently hydrogen, optionally substituted alkyl etc; R8 and R9 are independently hydrogen, optionally substituted alkyl etc; R10 and R11 are independently hydrogen, alkyl etc.
    Type: Grant
    Filed: March 22, 2001
    Date of Patent: June 10, 2003
    Assignee: Sumitomo Pharmaceuticals Co., Ltd.
    Inventors: Teruhisa Tokunaga, Takashi Umezome, W. Ewan Hume, Ryu Nagata, Kazuhiko Okazaki, Yasuyuki Ueki, Kazuo Kumagai
  • Patent number: 6569888
    Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt, in vivo hydrolysable ester, or an N—C1-6alkyl or N,N-di-(C1-6alkyl)amide thereof, where X is CH2 or SO2; R1 is an aryl optionally substituted by alkyl, alkenyl, alkynyl, halo, haloalkyl including perhaloalkyl such as trifluoromethyl, mercapto, alkoxy, haloalkoxy, alkenyloxy, alkynyloxy, hydroxyalkoxy, alkoxyalkoxy, alkanoyl, alkanoyloxy, cyano, nitro, amino, mono- or di-alkyl amino, oximino, sulphonamido, carbamoyl, mono or dialkylcarbamoyl or S(O)mR21 where m is defined above and R21 is hydrocarbyl; R4 is a group OR15 or S(O)qR15, where q is 0, 1 or 2 and R15 is a hydrogen-containing alkyl group substituted by at least one functional group as defined below, or an aryl group which is optionally substituted by one or more functional groups as defined below; and R2, R3, R5, R6 and R7 are specified organic groups.
    Type: Grant
    Filed: September 12, 2001
    Date of Patent: May 27, 2003
    Assignee: AstraZeneca AB
    Inventors: Jason Kettle, Alan W Faull
  • Patent number: 6570023
    Abstract: A process for preparing novel compounds useful in the preparation of 1H-indole-3-glyoxamides.
    Type: Grant
    Filed: March 19, 2001
    Date of Patent: May 27, 2003
    Assignee: Eli Lilly and Company
    Inventors: Benjamin Alan Anderson, Nancy Kay Harn, Richard Duane Miller, Edward Francis Plocharczyk
  • Publication number: 20030087949
    Abstract: The invention provides a compound represented by the following formula (I) useful for inhibiting death of cells, the drug being expected as a preventive or a remedy for the progress of various diseases wherein cell death participates in progress and exacerbation thereof: 1
    Type: Application
    Filed: September 26, 2002
    Publication date: May 8, 2003
    Inventors: Mikiko Sodeoka, Miho Kato, Rei Asakai
  • Publication number: 20030069424
    Abstract: Indolylmaleimide derivatives comprising either a substituted phenyl, naphthyl, tetrahydronaphthyl, quinazolinyl, quinolyl, isoquinolyl or pyrimidinyl residue have interesting pharmaceutical properties, e.g. in the treatment and/or prevention of T-cell mediated acute or chronic inflammatory diseases or disorders, autoimmune diseases, graft rejection or cancer.
    Type: Application
    Filed: November 5, 2001
    Publication date: April 10, 2003
    Inventors: Rainer Albert, Nigel Graham Cooke, Sylvain Cottens, Claus Ehrhardt, Jean-Pierre Evenou, Richard Sedrani, Peter Von Matt, Jurgen Wagner, Gerhard Zenke
  • Publication number: 20030045565
    Abstract: The present invention is directed to 1-pyrrolidin-1-ylmethyl-3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives that modulate the activity of protein kinases (“PKs”). Pharmaceutical compositions comprising these compounds, methods of treating diseases related to abnormal PK activity utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.
    Type: Application
    Filed: September 16, 2002
    Publication date: March 6, 2003
    Applicant: Pharmacia & Upjohn Company
    Inventors: Malcolm Wilson Moon, Walter Morozowich, Ping Gao
  • Patent number: 6528658
    Abstract: A series of steps of (A) a step for bringing a cycloalkane into contact with molecular oxygen (oxidizing reactor 2) in the presence of an oxidizing catalyst having an imide unit of the following formula (I): wherein X represents oxygen atom or hydroxyl group; (B) a step for separating the catalyst, and by-produced acid component or a derivative thereof from the reaction mixture (filter 3, extracting column 4, hydrolyzing unit 7, saponifying unit 8); and (C) steps for separating the cycloalkane, a cycloalkanol, and a cycloalkanone from the reaction mixture individually (distilling columns 5, 6, 9, and 10) makes it possible to produce cycloalkanones efficiently. A first component (lower-boiling point component) containing the cycloalkane and a second component (higher-boiling point component) containing the cycloalkanone and cycloalkanol may be separated from the reaction mixture, and the cycloalkanone and the cycloalkanol may be separated from the higher-boiling point component.
    Type: Grant
    Filed: October 18, 2000
    Date of Patent: March 4, 2003
    Assignee: Daicel Chemical Industries, Ltd.
    Inventors: Hiroyuki Miura, Hitoshi Watanabe, Tomohide Ina, Hidehiko Nakajima
  • Patent number: 6521657
    Abstract: This invention relates to compounds which are agonists of the progesterone receptor which have the general structure: wherein: R1, R2, R3, R4, R5 and Q1 are as defined herein, or a pharmaceutically acceptable salt thereof, as well as methods of using these compounds to induce contraception or treat progesterone-related carcinomas and adenocarcinomas.
    Type: Grant
    Filed: October 30, 2001
    Date of Patent: February 18, 2003
    Assignees: Wyeth, Ligand Pharmaceuticals, Inc.
    Inventors: Andrew Fensome, Puwen Zhang, Marci C. Koko, Lin Zhi, Todd K. Jones, Jay E. Wrobel, Christopher M. Tegley, James P. Edwards, Edward G. Melenski