The Additional Hetero Ring Is Bonded Directly To A Ring Carbon Of The Bicyclo Ring System Patents (Class 548/466)
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Publication number: 20080242675Abstract: This invention relates to PKC inhibitors which are able to selectively inhibit e.g. the and optionally 0, isoforms of PKC, and their use in particular in transplantation.Type: ApplicationFiled: January 19, 2005Publication date: October 2, 2008Inventors: Maurice Van Eis, Peter Von Matt, Jurgen Wagner, Jean-Pierre Evenou, Walter Schuler
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Publication number: 20080234494Abstract: 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: ApplicationFiled: January 19, 2005Publication date: September 25, 2008Inventors: Maurice Van Eis, Peter Von Matt, Jurgen Wagner, Jean-Pierre Evenou
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Publication number: 20080227842Abstract: 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: ApplicationFiled: March 11, 2008Publication date: September 18, 2008Inventors: Bernhard Krautler, Thomas Muller
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Patent number: 7425553Abstract: 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: GrantFiled: May 28, 2004Date of Patent: September 16, 2008Assignee: Gemin X Pharmaceuticals Canada inc.Inventors: Giorgio Attardo, Jean-Francois Lavallee, Elise Rioux, Terrence W. Doyle
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Publication number: 20080221160Abstract: 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: ApplicationFiled: March 4, 2008Publication date: September 11, 2008Applicant: WyethInventors: Casey Cameron McComas, Andrew Fensome
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Patent number: 7405300Abstract: 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: GrantFiled: September 1, 2004Date of Patent: July 29, 2008Assignee: Aventis Pharmaveuticals Inc.Inventors: John Z. Jiang, Jack Roger Koehl, Shujaath Mehdi, Neil David Moorcroft, Kwon Yon Musick, Philip Marvin Weintraub, Paul Robert Eastwood
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Publication number: 20080146587Abstract: 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: ApplicationFiled: November 8, 2007Publication date: June 19, 2008Inventors: Joe Timothy Bamberg, Counde O'Yang, Meng Sui, Shu-Hai Zhao
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Publication number: 20080119490Abstract: 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: ApplicationFiled: November 30, 2007Publication date: May 22, 2008Applicant: Boehringer Ingelheim International GmbHInventors: Marc-Andre POUPART, Pierre Louis BEAULIEU, Jean RANCOURT
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Patent number: 7375219Abstract: 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: GrantFiled: April 13, 2006Date of Patent: May 20, 2008Assignee: NeurAxon, Inc.Inventors: Shawn Maddaford, Jailall Ramnauth, Suman Rakhit, Joanne Patman, Paul Renton, Subhash C. Annedi
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Patent number: 7371868Abstract: 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: GrantFiled: March 27, 2007Date of Patent: May 13, 2008Assignee: Toyama Chemical Co., Ltd.Inventors: Katsuji Ojima, Tamotsu Takamatsu, Kyoko Taya, Taro Kiyoto
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Publication number: 20080045560Abstract: 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: ApplicationFiled: August 13, 2007Publication date: February 21, 2008Applicant: WyethInventors: Thomas Joseph Commons, Andrew Fensome, Gavin David Heffernan, Casey Cameron McComas, Richard Page Woodworth, Michael Byron Webb, Michael Anthony Marella, Edward George Melenski
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Publication number: 20080027122Abstract: 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: ApplicationFiled: July 26, 2007Publication date: January 31, 2008Inventors: Sumihiro Nomura, Shigeki Sakamaki
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Patent number: 7323470Abstract: 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: GrantFiled: April 17, 2006Date of Patent: January 29, 2008Assignee: Boehringer Ingelheim International GmbHInventors: Marc-André Poupart, Pierre Louis Beaulieu, Jean Rancourt
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Patent number: 7317037Abstract: 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: GrantFiled: July 6, 2005Date of Patent: January 8, 2008Assignee: WyethInventors: Andrew Fensome, Casey Cameron McComas, Edward George Melenski, Michael Anthony Marella, Jay Edward Wrobel, Gary Sondermann Grubb
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Publication number: 20070244125Abstract: 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: ApplicationFiled: April 5, 2007Publication date: October 18, 2007Inventors: Matthias Nettekoven, Jean-Marc Plancher, Hans Richter, Olivier Roche, Sven Taylor
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Patent number: 7282507Abstract: 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: GrantFiled: April 1, 2005Date of Patent: October 16, 2007Assignee: Janssen Pharmaceutica N.V.Inventors: James C. Lanter, Zhihua Sui, James J. Fiordeliso, Weiqin Jiang, Xuqing Zhang
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Patent number: 7271192Abstract: 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: GrantFiled: June 7, 2004Date of Patent: September 18, 2007Assignee: Gruenenthal GmbHInventors: Corinna Sundermann, Bernd Sundermann, Helmut Buschmann, Hagen-Heinrich Hennies
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Patent number: 7265148Abstract: The present invention relates generally to substituted pyrrole-indoles such as substituted pyrrole-indoles, and methods of using them.Type: GrantFiled: September 23, 2004Date of Patent: September 4, 2007Assignee: WyethInventor: Baihua Hu
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Patent number: 7253203Abstract: 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: GrantFiled: March 17, 2006Date of Patent: August 7, 2007Assignee: WyethInventors: 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
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Patent number: 7220774Abstract: 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: GrantFiled: September 11, 2003Date of Patent: May 22, 2007Assignee: Novartis AGInventors: Rainer Albert, Claus Ehrhardt, Jean-Pierre Evenou, Richard Sedrani, Peter Von Matt, Jurgen Wagner, Gerhard Zenke
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Patent number: 7202266Abstract: 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: GrantFiled: July 16, 2004Date of Patent: April 10, 2007Assignee: 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
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Patent number: 7202267Abstract: 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: GrantFiled: January 19, 2005Date of Patent: April 10, 2007Assignee: Sanofi-aventisInventors: Alain Aulombard, Georges Garcia, Antoine Pradines, Claudine Serradeil-Le Gal, Jean Wagnon
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Patent number: 7176200Abstract: 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 themType: GrantFiled: September 3, 2004Date of Patent: February 13, 2007Assignee: Laboratories Del Dr. Esteve, S.A.Inventors: Ramón Merce-Vidal, Blas Andaluz-Mataro, Jordi Frigola-Constansa
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Patent number: 7148240Abstract: 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: GrantFiled: August 23, 2001Date of Patent: December 12, 2006Assignee: Sanofi-AventisInventors: Jean-Louis Assens, Claude Bernhart, Frédérique Cabanel-Haudricourt, Dino Nisato
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Patent number: 7144912Abstract: 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: GrantFiled: July 18, 2002Date of Patent: December 5, 2006Assignee: Gemin X Biotechnologies Inc.Inventors: Roy A. Johnson, Giorgio Attardo
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Patent number: 7129240Abstract: 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: GrantFiled: April 29, 2004Date of Patent: October 31, 2006Assignee: Sanofi-AventisInventors: Richard Roux, Claudine Serradeil-le Gal, Bernard Tonnerre, Jean Wagnon
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Patent number: 7098231Abstract: 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 polymeraseType: GrantFiled: January 12, 2004Date of Patent: August 29, 2006Assignee: Boehringer Ingelheim International GmbHInventors: Marc-Andre Poupart, Pierre Louis Beaulieu, Jean Rancourt
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Patent number: 7094800Abstract: 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: GrantFiled: July 26, 2004Date of Patent: August 22, 2006Assignee: Sanofi-Aventis Deutschland GmbHInventors: Karl Schoenafinger, Holger Wagner, Gerhard Jaehne, Holger Gaul, Christian Buning, Georg Tschank, Ulrich Werner
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Patent number: 7087750Abstract: 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: GrantFiled: October 22, 2001Date of Patent: August 8, 2006Assignee: Biovitrum ABInventors: Patrizia Caldirola, Björn M. Nilsson, Gary Johansson
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Patent number: 7056932Abstract: 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: GrantFiled: December 10, 2004Date of Patent: June 6, 2006Assignee: Hoffman-La Roche Inc.Inventors: Luca Claudio Gobbi, Katrin Groebke Zbinden, Peter Mohr, Ulrike Obst
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Patent number: 7012088Abstract: The present invention provides antibacterial agents of formula I described herein and intermediates for their preparation.Type: GrantFiled: January 22, 2004Date of Patent: March 14, 2006Assignee: Pharmacia & Upjohn CompanyInventor: Toni-Jo Poel
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Patent number: 6900322Abstract: 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: GrantFiled: May 10, 1999Date of Patent: May 31, 2005Assignee: Solvay Pharmaceuticals GmbHInventors: Michael Reggelin, Timo Heinrich, Bernd Junker, Jochen Antel, Ulf Preuschoff
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Patent number: 6875770Abstract: 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: GrantFiled: October 1, 2003Date of Patent: April 5, 2005Assignee: Chugai Seiyaku Kabushiki KaishaInventors: Hiroharu Matsuoka, Nobuaki Kato, Tadakatsu Takahashi, Noriaki Maruyama, Takenori Ishizawa, Yukio Suzuki
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Patent number: 6787651Abstract: 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: GrantFiled: October 9, 2001Date of Patent: September 7, 2004Assignee: SmithKline Beecham CorporationInventors: 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
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Patent number: 6767912Abstract: 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: GrantFiled: December 20, 2001Date of Patent: July 27, 2004Assignee: WyethInventors: Ping Zhou, Derek Cecil Cole, Michael Gerard Kelly, William Joseph Lennox
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Patent number: 6750241Abstract: 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: GrantFiled: March 6, 2002Date of Patent: June 15, 2004Assignee: Theravance, Inc.Inventors: John H. Griffin, Yu-Hua Ji, Edmund J. Moran, Jonathan W. Wray
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Patent number: 6730695Abstract: 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: GrantFiled: July 24, 2002Date of Patent: May 4, 2004Assignee: Sanofi-SynthelaboInventors: Richard Roux, Claudine Serradeil-Le Gal, Bernard Tonnerre, Jean Wagnon
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Patent number: 6699886Abstract: 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: GrantFiled: May 31, 2002Date of Patent: March 2, 2004Assignee: Cellegy Pharmaceuticals, Inc.Inventors: Thomas P. Parks, Don R. Baker
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Patent number: 6689806Abstract: 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: GrantFiled: March 22, 2000Date of Patent: February 10, 2004Assignee: 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
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Patent number: 6673797Abstract: 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: GrantFiled: November 27, 2000Date of Patent: January 6, 2004Assignee: Chugai Seiyaku Kabushiki KaishaInventors: Hiroharu Matsuoka, Nobuaki Kato, Tadakatsu Takahashi, Noriaki Maruyama, Takenori Ishizawa, Yukio Suzuki
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Patent number: 6630463Abstract: 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: GrantFiled: July 23, 2001Date of Patent: October 7, 2003Assignee: 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
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Patent number: 6605633Abstract: 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: GrantFiled: May 16, 2002Date of Patent: August 12, 2003Assignee: Fournier Industrie et SanteInventors: Jean-Luc Paquet, Martine Barth, Didier Pruneau, Pierre Dodey
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Publication number: 20030121113Abstract: Oxobenzofuranylidene-dihydroindolones of formulae trans-(Ia) and cis-(Ib) 1Type: ApplicationFiled: December 18, 2002Publication date: July 3, 2003Inventors: Peter Nesvadba, Joachim Jandke
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Patent number: 6576656Abstract: 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: GrantFiled: March 22, 2001Date of Patent: June 10, 2003Assignee: Sumitomo Pharmaceuticals Co., Ltd.Inventors: Teruhisa Tokunaga, Takashi Umezome, W. Ewan Hume, Ryu Nagata, Kazuhiko Okazaki, Yasuyuki Ueki, Kazuo Kumagai
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Patent number: 6570023Abstract: A process for preparing novel compounds useful in the preparation of 1H-indole-3-glyoxamides.Type: GrantFiled: March 19, 2001Date of Patent: May 27, 2003Assignee: Eli Lilly and CompanyInventors: Benjamin Alan Anderson, Nancy Kay Harn, Richard Duane Miller, Edward Francis Plocharczyk
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Patent number: 6569888Abstract: 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: GrantFiled: September 12, 2001Date of Patent: May 27, 2003Assignee: AstraZeneca ABInventors: Jason Kettle, Alan W Faull
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Publication number: 20030087949Abstract: 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: 1Type: ApplicationFiled: September 26, 2002Publication date: May 8, 2003Inventors: Mikiko Sodeoka, Miho Kato, Rei Asakai
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Publication number: 20030069424Abstract: 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: ApplicationFiled: November 5, 2001Publication date: April 10, 2003Inventors: Rainer Albert, Nigel Graham Cooke, Sylvain Cottens, Claus Ehrhardt, Jean-Pierre Evenou, Richard Sedrani, Peter Von Matt, Jurgen Wagner, Gerhard Zenke
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Publication number: 20030045565Abstract: 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: ApplicationFiled: September 16, 2002Publication date: March 6, 2003Applicant: Pharmacia & Upjohn CompanyInventors: Malcolm Wilson Moon, Walter Morozowich, Ping Gao
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Patent number: 6528658Abstract: 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: GrantFiled: October 18, 2000Date of Patent: March 4, 2003Assignee: Daicel Chemical Industries, Ltd.Inventors: Hiroyuki Miura, Hitoshi Watanabe, Tomohide Ina, Hidehiko Nakajima