Chalcogen Bonded Directly To The Bicyclo Ring System Patents (Class 544/144)
  • 3-(4-amidopyrrol-2-ylmethlidene)-2-indolinone derivatives as protein kinase inhibitors
    Patent number: 7179910
    Abstract: The present invention relates to pyrrole substituted 2-indolinone compounds and their pharmaceutically acceptable salts which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.
    Type: Grant
    Filed: September 8, 2003
    Date of Patent: February 20, 2007
    Assignee: Agouron Pharmaceuticals, Inc.
    Inventors: Huiping Guan, Congxin Liang, Li Sun, Peng Cho Tang, Chung Chen Wei, Tomas Vojkovsky, Qingwu (Alan) Jin, Paul M. Herrinton, Michael A. Mauragis
  • Receptor selective cannabimimetic aminoalkylindoles
    Patent number: 7173027
    Abstract: Disclosed are cannabimimetic aminoalkylindole compounds and methos for their manufacture. The disclosed compounds are surprisingly potent and selective cannabinoinds. Also disclosed are methods of using the disclosed compounds, including use of the disclosed compounds to stimulate a cannabinoid receptor, to provide a physiological effect in an animal or individual and to treat a condition in an animal or individual.
    Type: Grant
    Filed: January 29, 2002
    Date of Patent: February 6, 2007
    Assignee: University of Connecticut
    Inventors: Alexandros Makriyannis, Hongfeng Deng
  • Polyamine analogues as therapeutic and diagnostic agents
    Patent number: 7160923
    Abstract: Novel inhibitors of polyamine transport having inhibition constants two orders of magnitude lower than those of known compounds are disclosed. These polyamine analogues are useful pharmaceutical agents for treating diseases where it is desired to inhibit polyamine transport or other polyamine binding proteins, for example cancer and post-angioplasty injury. Novel chemical synthetic methods to obtain polyamine analogues are disclosed, including the production of a combinatiorial polyamine library. These approaches yield analogues with desirable activities both for diagnostic and research assays and therapy. The assays of the invention are useful for high throughput screening of targets in the discovery of drugs that interact with the polyamine system.
    Type: Grant
    Filed: November 14, 2000
    Date of Patent: January 9, 2007
    Assignee: MediQuest Therapeutics, Inc.
    Inventors: Nicolaas M. J. Vermeulin, Christine L. O'Day, Heather K. Webb, Mark R. Burns, Donald E. Bergstrom
  • 5-sulfonamido-substituted indolinone compounds as protein kinase inhibitors
    Patent number: 7157577
    Abstract: The present invention relates to 5-sulfonamido substituted indolinones that modulate the activity of protein kinases (“PKs”). The compounds of this invention are therefore useful in treating disorders related to abnormal PK activity. Pharmaceutical compositions comprising these compounds, methods of treating diseases utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.
    Type: Grant
    Filed: March 8, 2004
    Date of Patent: January 2, 2007
    Assignee: Sugen Inc.
    Inventors: Peng Cho Tang, Congxin Liang, Todd Miller, Kenneth E. Lipson
  • Indolinones substituted by heterocycles, the preparation thereof and their use as medicaments
    Patent number: 7148249
    Abstract: The present invention relates to heterocyclically substituted indolinones of general formula wherein R1 to R5 and X are defined as in claim 1, the tautomers, the diastereomers, the enantiomers, the mixtures thereof, the prodrugs thereof and the salts thereof, particularly the physiologically acceptable salts thereof which have valuable pharmacological properties, in particular an inhibiting effect on various receptor tyrosine kinases and cyclin/CDK complexes and on the proliferation of endothelial cells and various tumour cells, pharmaceutical compositions containing these compounds, their use and processes for preparing them.
    Type: Grant
    Filed: September 5, 2003
    Date of Patent: December 12, 2006
    Assignee: Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Joerg Kley, Frank Hilberg, Armin Heckel, Gerald Juergen Roth, Thorsten Lehmann-Lintz, Ralf R. H. Lotz, Ulrike Tontsch-Grunt, Jacobus C. A. Van Meel
  • 1,3-dihydro-2H-indol-2one derivatives, process for preparing them and pharmaceutical compositions containing them
    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
  • Pyrrole substituted 2-indolinone protein kinase inhibitors
    Patent number: 7119090
    Abstract: The present invention relates to novel pyrrole substituted 2-indolinone compounds and physiologically acceptable salts and prodrugs thereof which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.
    Type: Grant
    Filed: February 25, 2002
    Date of Patent: October 10, 2006
    Assignee: Sugen, Inc.
    Inventors: Peng Cho Tang, Li Sun, Gerald McMahon
  • Cyclohept[b]indole derivatives
    Patent number: 7109231
    Abstract: A novel class of tricyclic compounds of the following formula (I): (formula I); is disclosed together with the use of such compounds for inhibiting sPLA2 mediated release of fatty acids for treatment of inflammatory diseases such as septic shock
    Type: Grant
    Filed: July 29, 2002
    Date of Patent: September 19, 2006
    Assignee: Eli Lilly and Company
    Inventors: Michael Dean Kinnick, Edward David Mihelich, John Michael Morin, Jr., Daniel Jon Sall, Jason Scott Sawyer
  • Indolinone derivatives as protein kinase/phosphatase inhibitors
    Patent number: 7071332
    Abstract: The present invention relates to certain 2-indolinone compounds which modulate the activity of protein kinases (“PKs”) and phosphatases. The compounds of this invention are therefore useful in treating disorders related to abnormal PK activity. Pharmaceutical compositions comprising these compounds, methods of treating diseases utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.
    Type: Grant
    Filed: December 2, 2003
    Date of Patent: July 4, 2006
    Assignee: Sugen, Inc.
    Inventors: Peng Cho Tang, G. Davis Harris, Xiaoyuan Li
  • Indolinone derivatives
    Patent number: 7060703
    Abstract: Compounds of formula (I) in which R1, R2, R3 and R4 have the meanings given in the specification, are receptor tyrosine kinase inhibitors useful in the treatment of proliferative disorders, such as cancer.
    Type: Grant
    Filed: October 22, 2003
    Date of Patent: June 13, 2006
    Assignee: Theravance, Inc.
    Inventors: John H. Griffin, Roger Briesewitz, Jonathan W. Wray
  • 3-(arylamino)methylene-1, 3-dihydro-2H-indol-2-ones as kinase inhibitors
    Patent number: 7015220
    Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.
    Type: Grant
    Filed: February 20, 2004
    Date of Patent: March 21, 2006
    Assignee: Allergan, Inc.
    Inventors: Steven W. Andrews, Julie A. Wurster, Edward H. Wang, Thomas Malone
  • Nitriles useful as reversible inhibitors of cysteine proteases
    Patent number: 6982263
    Abstract: Disclosed are novel nitrile compounds of formula (I) further defined herein, which compounds are useful as reversible inhibitors of cysteine proteases such as cathepsin K, S, F, L and B. These compounds are useful for treating diseases and pathological conditions exacerbated by these proteases such as, but not limited to, osteoporosis, rheumatoid arthritis, multiple sclerosis, asthma and other autoimmune diseases, Alzheimer's disease, atherosclerosis. Also disclosed are processes for making such novel compounds.
    Type: Grant
    Filed: June 4, 2002
    Date of Patent: January 3, 2006
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Eugene R. Hickey, Younes Bekkali, Usha R. Patel, Denice Mary Spero, David S. Thomson, Erick Richard Roush Young
  • Substituted isoindoles and the use thereof
    Patent number: 6933295
    Abstract: The invention relates to the field of blood clotting, to novel compounds of formula (I), to a method for their production and to the use of these compounds as active ingredients in medicaments for preventing and/or treating diseases. The compounds are factor Xa inhibitors.
    Type: Grant
    Filed: July 3, 2002
    Date of Patent: August 23, 2005
    Assignee: Bayer Aktiengesellschaft
    Inventors: Alexander Straub, Thomas Lampe, Jens Pohlmann, Susanne Röhrig, Stephan Jordan, Elisabeth Perzborn, Karl-Heinz Schlemmer
  • Substituted indolines with an inhibitory effect on various kinases and complexes of CDKs
    Patent number: 6855710
    Abstract: The present invention relates to new substituted indolinones of general formula wherein X and R1 to R5 are defined as in claim 1, the isomers and the salts thereof which have valuable properties. The above compounds of general formula I wherein R1 denotes a hydrogen atom, a C1-3-alkyl group or a prodrug group have valuable pharmacological properties, particularly an inhibiting effect on various kinases, on viral cyclin and on receptor tyrosine kinases, and the other compounds of the above general formula I wherein R1 does not represent a hydrogen atom, a C1-3-alkyl group or a prodrug group are valuable intermediate products for the preparation of the abovementioned compounds.
    Type: Grant
    Filed: September 19, 2003
    Date of Patent: February 15, 2005
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Rainer Walter, Wolfgang Grell, Armin Heckel, Frank Himmelsbach, Wolfgang Eberlein, Gerald Roth, Jacobus C.A. van Meel, Norbert Redemann, Walter Spevak, Ulrike Tontsch-Grunt, Thomas von Rueden
  • 3-methylidenyl-2-indolinone modulators of protein kinase
    Patent number: 6855730
    Abstract: The present invention relates to novel 3-methylidenyl-2-indolinone compounds and physiologically acceptable salts and prodrugs thereof which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.
    Type: Grant
    Filed: March 10, 2003
    Date of Patent: February 15, 2005
    Assignee: Sugen, Inc.
    Inventors: Pen Cho Tang, Li Sun, Todd Anthony Miller, Congxin Liang, Ngoc My Tran, Anh Thi Nguyen, Asaad Nematalla
  • Selective inhibitors of cyclooxygenase-2
    Patent number: 6846818
    Abstract: The present invention relates to cyclooxygenase-2 (COX-2) selective inhibitors of formula I: pharmaceutical compositions containing them, to their medicinal use, and to their preparations. The compounds of the invention are particularly useful in the treatment or alleviation of inflammation and inflammation associated disorders, such as, for example, rheumatoid arthritis and osteoarthritis, and in the relief of pain, such as, for example, pain associated with surgery or trauma, in mammals, preferably felines and canines.
    Type: Grant
    Filed: April 16, 2003
    Date of Patent: January 25, 2005
    Assignee: Pfizer Inc.
    Inventors: Kristin Lundy DeMello, Brian S. Bronk, Rhonda Marie Crosson
  • Fluorescent group-containing carbodiimide compound and process for producing the compound
    Patent number: 6825195
    Abstract: A novel carbodiimide compound represented by the general formula (1) having an ester linkage and containing a fluorescent group can be prepared for providing a novel carbodiimide compound and a process for producing such a compound, in which the fluorescent group of such a compound can be efficiently introduced into a nucleic acid including a naturally-occurring nucleic acid or into a protein in a simple manner, while retaining a sufficient solubility to water. In addition, a fluorescent group-containing compound and a carbodiimide compound which can be efficiently coupled together in a simple manner.
    Type: Grant
    Filed: May 21, 2002
    Date of Patent: November 30, 2004
    Assignee: Nisshinbo Industries, Inc.
    Inventor: Naoki Kimura
  • Indole derivatives, process for preparation of the same and use thereof
    Publication number: 20040180885
    Abstract: Indole derivatives represented by formula (I): 1
    Type: Application
    Filed: March 8, 2004
    Publication date: September 16, 2004
    Applicant: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Kazuhiko Torisu, Kaoru Kobayashi, Fumio Nambu
  • Process for synthesis of heteroaryl-substituted urea compounds useful as antiinflammatory agents
    Patent number: 6774233
    Abstract: Disclosed are novel processes and novel intermediate compounds for preparing aryl- and heteroaryl-substituted urea compounds of the formula(I) wherein Ar1, Ar2, L, Q and X are described herein. The product compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases.
    Type: Grant
    Filed: February 10, 2003
    Date of Patent: August 10, 2004
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Lin-Hua Zhang, Lei Zhu
  • 1-sulfonyl-4-aminoalkoxy indole derivatives and uses thereof
    Patent number: 6774241
    Abstract: The present invention provides a compound of the formula: a pharmaceutically acceptable salt or a prodrug thereof, where R1, R2, R3, R4, R5, R6, and n are as defined herein. The present invention also provides compositions comprising, methods for using, and methods for preparing Compound of Formula I.
    Type: Grant
    Filed: June 4, 2003
    Date of Patent: August 10, 2004
    Assignee: Roche Palo Alto LLC
    Inventors: Robin Douglas Clark, Shu-Hai Zhao
  • Substituted indolines which inhibit receptor tyrosine kinases
    Patent number: 6762180
    Abstract: Indolinones of the formula having an inhibitory effect on receptor tyrosine kinases and cyclin/CDK complexes, as well as on the proliferation of endothelial cells and various tumor cells. Exemplary are: (a) 3-Z-[1-(4-(piperidin-1-yl-methyl)-anilino)-1-phenyl-methylene]-6-ethoxycarbonyl-2-indolinone, (b) 3-Z-[(1-(4-(piperidin-1-yl-methyl)-anilino)-1-phenyl-methylene]-6-carbamoyl-2-indolinone, and (c) 3-Z-[1-(4-(piperidin-1-yl-methyl)-anilino)-1-phenyl-methylene]-6-metboxycarbonyl-2-indolinone.
    Type: Grant
    Filed: October 3, 2000
    Date of Patent: July 13, 2004
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Gerald Juergen Roth, Armin Heckel, Rainer Walter, Jacobus Van Meel, Norbert Redemann, Ulrike Tontsch-Grunt, Walter Spevak, Frank Hilberg
  • Kinase inhibitors for the treatment of disease
    Patent number: 6747025
    Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell poliferation.
    Type: Grant
    Filed: March 13, 2003
    Date of Patent: June 8, 2004
    Assignee: Allergan, Inc.
    Inventors: Steven W. Andrews, Michael E. Garst, Xialing Guo, Jonathan J. Hebert, Thomas Malone, Julie A. Wurster, Clarence Eugene Hull, III
  • Inhibitors of cyclin-dependent kinases and their use
    Publication number: 20040106581
    Abstract: The present invention relates to novel compounds for the inhibition of cyclin-dependent kinases, and more particularly, to chromenone derivatives of formula (Ia), 1
    Type: Application
    Filed: July 1, 2003
    Publication date: June 3, 2004
    Inventors: Bansi Lal, Kalpana Joshi, Sanjeev Kulkarni, Malcolm Mascarenhas, Shrikant Kamble, Maggie Joyce Rathos, Rajendrakumar Joshi
  • 4-heteroaryl-3-heteroarylidenyl-2-indolinones and their use as protein kinase inhibitors
    Publication number: 20040097497
    Abstract: The present invention relates to certain 4-heteroaryl-3-heteroarylidenyl-2-indolinones compounds and their physiologically acceptable salts which modulate the activity of protein kinases (“PKs”), in particular CDK2. The compounds of the present invention are therefore useful in treating disorders related to abnormal PK activity. Pharmaceutical composition containing these compounds and methods of preparing these compounds are also described.
    Type: Application
    Filed: August 27, 2003
    Publication date: May 20, 2004
    Applicant: Sugen, Inc.
    Inventors: Peng Cho Tang, Chung Chen Wei, Ping Huang, Jingrong Cui
  • Pigmented vitreous material
    Patent number: 6737533
    Abstract: The present application relates to a process for the manufacture of pigmented vitreous materials, as well as to pigmented vitreous materials, characterized by the use of soluble pigment precursors and preferably the absence of significant amounts of dispersants. These pigmented vitreous materials can be used as coloured materials for any known purposes. Soluble pigment precursors comprising a partial structure: are also claimed, wherein X1 is an aromatic or heteroaromatic ring, B is hydrogen or a group of the formula: but at least one group B is not hydrogen, and L is a solubilizing group.
    Type: Grant
    Filed: January 2, 2003
    Date of Patent: May 18, 2004
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: Véronique Hall-Goulle, Zhimin Hao
  • 1-(aminoalkyl)-3-sulfonylindole-and-indazole derivatives as 5-hydroxytryptamine-6 ligands
    Patent number: 6727246
    Abstract: The present invention provides compounds of formula I and the use thereof for the treatment of central nervous system disorders related to or affected by the 5-HT6 receptor.
    Type: Grant
    Filed: June 3, 2003
    Date of Patent: April 27, 2004
    Assignee: Wyeth
    Inventors: Ronald Charles Bernotas, Steven Edward Lenicek, Schuyler A. Antane, Ping Zhou, Yanfang Li
  • Guanidino compounds
    Patent number: 6716840
    Abstract: Compounds having the general structure I are provided: X and Y are independently selected from the group consisting of CH2, N, NR9, C═O, C═S, S═O, SO2, S, O, (CR6R7)n, C(═O)—(CR6R7)n, and C(═S)—(CR6R7)n, where n is 1, 2, or 3. W is selected from the group consisting of and L is selected from the group consisting of N, O, S, S═O, SO2, C(O), NC(O), NC(S), OC(O), OC(S), C(NR10), C(NOR10), and a covalent bond. Z1, Z2, and Z3 are independently selected from the group consisting of substituted carbon and nitrogen. Compounds of formula I are agonists of the melanocortin-4 receptor (“MC-4r”) and therefore may have useful properties for controlling diseases related to MC-4r action in humans, such as obesity and type II diabetes.
    Type: Grant
    Filed: April 8, 2002
    Date of Patent: April 6, 2004
    Assignee: Chiron Corporation
    Inventors: Daniel Chu, Rustum S. Boyce, David Duhl, Bryan H. Chang
  • Indolinone derivatives as protein kinase/phosphatase inhibitors
    Patent number: 6706709
    Abstract: The present invention relates to certain 2-indolinone compounds which modulate the activity of protein kinases (“PKs”) and phosphatases. The compounds of this invention are therefore useful in treating disorders related to abnormal PK activity. Pharmaceutical compositions comprising these compounds, methods of treating diseases utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.
    Type: Grant
    Filed: June 4, 2001
    Date of Patent: March 16, 2004
    Assignee: Sugen, Inc.
    Inventors: Peng Cho Tang, G. Davis Harris, Xiaoyuan Li
  • Kinase inhibitors for the treatment of disease
    Patent number: 6699863
    Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.
    Type: Grant
    Filed: November 27, 2002
    Date of Patent: March 2, 2004
    Assignee: Allergan, Inc.
    Inventors: Steven W. Andrews, Jonathan J. Hebert
  • Indolinone derivatives
    Patent number: 6686362
    Abstract: Compounds of formula (I) in which R1, R2, R3 and R4 have the meanings given in the specification, are receptor tyrosine kinase inhibitors useful in the treatment of proliferative disorders, such as cancer.
    Type: Grant
    Filed: December 20, 2002
    Date of Patent: February 3, 2004
    Assignee: Theravance, Inc.
    Inventors: John H. Griffin, Roger Briesewitz, Jonathan W. Wray
  • Indolin-2-one derivatives, preparation and their use as ocytocin receptor ligands
    Patent number: 6673790
    Abstract: The present invention relates to novel indolin-2-one derivatives of formula: to the preparation and to the pharmaceutical compositions comprising them. These compounds have an affinity for oxytocin receptors.
    Type: Grant
    Filed: October 2, 2002
    Date of Patent: January 6, 2004
    Assignee: Sanofi-Synthelabo
    Inventors: Loïc Foulon, Georges Garcia, Claudine Serradeil-Le Gal, Gérard Valette
  • 1-(AMINOALKYL)-3-SULFONYLINDOLE AND-INDAZOLE DERIVATIVES AS 5-HYDROXYTRYPTAMINE-6 LIGANDS
    Publication number: 20030232828
    Abstract: The present invention provides compounds of formula I and the use thereof for the treatment of central nervous system disorders related to or affected by the 5-HT6 receptor.
    Type: Application
    Filed: June 3, 2003
    Publication date: December 18, 2003
    Applicant: Wyeth
    Inventors: Ronald Charles Bernotas, Steven Edward Lenicek, Schuyler A. Antane, Ping Zhou, Yanfang Li
  • Phthalimido derivatives and a process for their preparation
    Patent number: 6660736
    Abstract: This invention relates to phthalimido derivatives of the formula wherein X is —N═ or —CH═, and R1 to R4 and m are as defined in the specification, as well as their pharmaceutically acceptable salts. The invention further relates to pharmaceutical compositions containing these compounds, a method of treating a disease by administering a therapeutically effective amount of at least one of these compounds, and a process for their preparation for the treatment or prevention of diseases in which MAO-B inhibitors might be beneficial.
    Type: Grant
    Filed: March 13, 2003
    Date of Patent: December 9, 2003
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Andrea Cesura, Rosa Maria Rodriguez Sarmiento, Andrew William Thomas, Rene Wyler
  • 3-(4-amidopyrrol-2-ylmethylidene)-2-indolinone derivatives as protein kinase inhibitors
    Patent number: 6653308
    Abstract: The present invention relates to pyrrole substituted 2-indolinone compounds and their pharmaceutically acceptable salts which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.
    Type: Grant
    Filed: February 15, 2002
    Date of Patent: November 25, 2003
    Assignees: Sugen, Inc., Pharmacia & Upjohn Company
    Inventors: Huiping Guan, Congxin Liang, Li Sun, Peng Cho Tang, Chung Chen Wei, Tomas Vojkovsky, Qingwu Jin, Paul M. Herrinton, Michael A. Mauragis
  • Tricyclic compounds
    Publication number: 20030216571
    Abstract: The present invention is to provide novel tricyclic compounds having leukotriene antagonistic action and represented by the formula: 1
    Type: Application
    Filed: July 31, 2002
    Publication date: November 20, 2003
    Inventors: Yoshiaki Kuroki, Hitoshi Ueno, Tetsushi Katsube, Tetsuo Kawaguchi, Eiji Okanari, Takashi Ikuta
  • Silver halide color photographic light-sensitive material, pyrrolotriazole compound and dye-forming compound
    Patent number: 6649771
    Abstract: A pyrrolotriazole compound of the following formula (I), and a silver halide color photographic light-sensitive material containing the pyrrolotriazole compound as a cyan coupler: wherein R1 and R2 each independently are an alkyl, cycloalkyl, alkenyl, aryl or heterocyclic group, provided that R1 and R2 may bond together to form a 5- or 6-membered nitrogen-containing heterocycle; R3 is an alkyl, cycloalkyl, alkenyl, aryl or heterocyclic group; R4 is an alkyl, cycloalkyl, alkenyl, alkoxy or amino group; R5 is a hydrogen atom, an alkyl or aryl group; R6 is an alkyl, cycloalkyl or alkenyl group; and X is an oxygen or sulfur atom.
    Type: Grant
    Filed: March 26, 2001
    Date of Patent: November 18, 2003
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Takeshi Nakamine, Nobuo Seto, Hideaki Sato, Yasuaki Deguchi
  • 3-[4-Substituted heterocyclyl)-pyrrol-2-ylmethylidene]-2- indolinone derivatives as kinase inhibitors
    Patent number: 6642232
    Abstract: The present invention relates to certain 3-[4-(substituted heterocyclyl)-pyrrol-2-ylmethylidene]-2-indolinone derivatives that inhibit kinases, in particular VEGFR and/or PDGFR kinases. Pharmaceutical compositions comprising these compounds, methods of treating diseases mediated by kinases utilizing pharmaceutical compositions comprising these compounds, and methods of preparing them are also disclosed.
    Type: Grant
    Filed: October 10, 2002
    Date of Patent: November 4, 2003
    Assignee: Sugen, Inc.
    Inventors: Matthew Mattson, Tomas Vojkovsky, Congxin Liang, Peng Cho Tang, Huiping Guan
  • 3-(Arylamino)methylene-1, 3-dihydro-2H-indol-2-ones as kinase inhibitors
    Publication number: 20030199478
    Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.
    Type: Application
    Filed: September 27, 2002
    Publication date: October 23, 2003
    Inventors: Steven W. Andrews, Julie A. Wurster, Edward H. Wang, Thomas Malone
  • PHTHALIMIDO DERIVATIVES AND A PROCESS FOR THEIR PREPARATION
    Publication number: 20030195208
    Abstract: This invention relates to phthalimido derivatives of the formula 1
    Type: Application
    Filed: March 13, 2003
    Publication date: October 16, 2003
    Inventors: Andrea Cesura, Rosa Maria Rodriguez Sarmiento, Andrew William Thomas, Rene Wyler
  • 1,3-dihydro-2H-indol-2-one derivatives, preparation method and pharmaceutical composition containing them
    Patent number: 6624164
    Abstract: The invention relates to compounds of formula: and their solvates and/or hydrates exhibiting affinity for the arginine-vasopressin V1b receptors or for both V1b and V1a receptors. The invention also relates to their process of preparation, to the intermediate compounds of formula (II) of use for their preparation, to the pharmaceutical compositions comprising them and to their use for the preparation of medicaments.
    Type: Grant
    Filed: November 25, 2002
    Date of Patent: September 23, 2003
    Assignee: Sanofi-Synthelabo
    Inventors: Bruno Schoentjes, Claudine Serradeil-Le Gal, Jean Wagnon
  • Indolinone derivatives
    Publication number: 20030171378
    Abstract: Compounds of formula (I) 1
    Type: Application
    Filed: December 20, 2002
    Publication date: September 11, 2003
    Inventors: John H. Griffin, Roger Briesewitz, Jonathan W. Wray
  • Fatty acid synthase inhibitors
    Patent number: 6608059
    Abstract: This invention relates to the use of compounds as inhibitors of the fatty acid synthase FabH.
    Type: Grant
    Filed: December 13, 2002
    Date of Patent: August 19, 2003
    Assignee: SmithKline Beecham Corporation
    Inventors: Robert A. Daines, Israil Pendrak
  • Indole sPLA2 inhibitors
    Patent number: 6608099
    Abstract: A class of novel acylsulfonamide substituted indole compounds is disclosed together with the use of such compounds for inhibiting sPLA2 mediated release of fatty acids for treatment of inflammatory diseases.
    Type: Grant
    Filed: January 30, 2001
    Date of Patent: August 19, 2003
    Assignee: Eli Lilly and Company
    Inventors: Edward David Mihelich, Michael LeRoy Phillips, Alan M Warshawsky
  • Fused pyrrolecarboxamides; a new class of GABA brain receptor ligands
    Publication number: 20030153754
    Abstract: Disclosed are the compounds of the formula: 1
    Type: Application
    Filed: November 22, 2002
    Publication date: August 14, 2003
    Applicant: Neurogen Corporation, A Corporation of the State of Delaware
    Inventors: Pamela Albaugh, Gang Liu, Kenneth Shaw, Alan Hutchison
  • 5-aralkysufonyl-3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives as kinase inhibitors
    Patent number: 6599902
    Abstract: The present invention relates to certain 5-aralkylsulfonyl-3-(pyrrol-2-yl-methylidene)-2-indolinone derivatives that inhibit kinases, in particular met kinase. Pharmaceutical compositions comprising these compounds, methods of treating diseases mediated by kinases utilizing pharmaceutical compositions comprising these compounds, and methods of preparing them are also disclosed.
    Type: Grant
    Filed: May 30, 2002
    Date of Patent: July 29, 2003
    Assignee: Sugen, Inc.
    Inventors: Jingrong Cui, John Ramphal, Congxin Liang, Connie Li Sun, Chung Chen Wei, Peng Cho Tang
  • Inhibitors of factor Xa
    Publication number: 20030114448
    Abstract: Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.
    Type: Application
    Filed: May 28, 2002
    Publication date: June 19, 2003
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Penglie Zhang, Bing-Yan Zhu, Wenrong Huang, Robert M. Scarborough
  • Oxindole derivative
    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
  • Pyrrole substituted 2-indolinone protein kinase inhibitors
    Patent number: 6573293
    Abstract: The present invention relates to pyrrole substituted 2-indolinone compounds and their pharmaceutically acceptable salts which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.
    Type: Grant
    Filed: February 15, 2001
    Date of Patent: June 3, 2003
    Assignees: Sugen, Inc., Pharmacia & Upjohn Co.
    Inventors: Peng Cho Tang, Todd A. Miller, Xiaoyuan Li, Li Sun, Chung Chen Wei, Shahrzad Shirazian, Congxin Liang, Tomas Vojkovsky, Asaad S. Nematalla, Michael Hawley
  • Prodrugs of a 3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives
    Publication number: 20030100555
    Abstract: The present invention relates to pyrrole substituted 2-indolinone compounds and their pharmaceutically acceptable salts which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.
    Type: Application
    Filed: April 9, 2002
    Publication date: May 29, 2003
    Applicant: Sugen. Inc.
    Inventors: Connie Li Sun, Chung Chen Wei, Peng Cho Tang, Marcel Koenig, Yong Zhou, Tomas Vojkovsky, Asaad S. Nematalla
  • 7-Substituted isoindolinone inhibitors of inflammation and reperfusion injury and methods of use thereof
    Patent number: 6534651
    Abstract: The invention provides a novel class of substituted isoindolinone derivatives, useful for the treatment of inflammation and reperfusion injuries. Pharmaceutical compositions, and methods of making and using the compounds, or pharmaceutically acceptable salts, hydrates, stereoisomers or mixtures thereof are also described. The novel isoindolinone derivatives have the formula: or a pharmaceutically acceptable base or acid addition salt, hydrate, stereoisomer, or mixtures thereof, wherein R14 is described herein.
    Type: Grant
    Filed: January 19, 2001
    Date of Patent: March 18, 2003
    Assignee: Inotek Pharmaceuticals Corp.
    Inventors: Prakash Jagtap, Garry Southan, Andrew Salzman, Csaba Szabo, Siya Ram