Three Or More Ring Hetero Atoms In The Bicyclo Ring System Patents (Class 544/91)
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Publication number: 20110028465Abstract: Compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.Type: ApplicationFiled: January 9, 2009Publication date: February 3, 2011Inventors: Matthew Duncton, Donogh John Roger O'Mahony, Matthew Cox, Maria De Los Angeles Estiarte-Martinez
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Publication number: 20110028466Abstract: The current invention pertains to nitroimidazooxazine and nitroimidazooxazole analogues, their methods of preparation, and uses of the compounds as treatment for Mycobacterium tuberculosis, for use as anti-tubercular drugs, for use as anti-protozoal agents with unexpectedly high potency against Trypanosoma cruzi or Leishmania donovani, and for the treatment of other microbial infections.Type: ApplicationFiled: July 30, 2010Publication date: February 3, 2011Applicant: Global Alliance for TB Drug DevelopmentInventors: Andrew Mark Thompson, William Alexander Denny, Adrian Blaser, Zhenkun Ma
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Publication number: 20110021492Abstract: The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein the variables A, L1, L2, R2, R11, and M are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of fXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.Type: ApplicationFiled: March 12, 2009Publication date: January 27, 2011Inventors: James R. Corte, Zilun HU, Mimi L. Quan
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Publication number: 20110021772Abstract: The invention relates to new heterocyclic compounds of general formula (I), and their salts with a base or an acid: The invention also relates to a process for the preparation of these compounds as well as their use as medicaments, in particular as anti-bacterial agents.Type: ApplicationFiled: April 16, 2010Publication date: January 27, 2011Inventors: Maxime Lampilas, Jozsef Aszodi, David Alan Rowlands, Claude Fromentin
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Publication number: 20100317657Abstract: The invention relates to the use of 1H-imidazo[4,5-c]quinolinone derivatives and salts thereof in the treatment of protein and/or lipid kinase dependent diseases and for the manufacture of pharmaceutical preparations for the treatment of said diseases; 1H-imidazo[4,5-c]quinolinone derivatives for use in the treatment of protein and/or lipid kinase dependent diseases; a method of treatment against said diseases, comprising administering the 1H-imidazo[4,5-c]quinolinone derivatives to a warm-blooded animal, especially a human; pharmaceutical preparations comprising an 1H-imidazo[4,5-c]quinolinone derivative, especially for the treatment of a protein and/or lipid kinase dependent disease; novel 1H-imidazo[4,5-c]quinolinone derivatives; and a process for the preparation of the novel 1H-imidazo[4,5-c]quinolinone derivatives.Type: ApplicationFiled: June 2, 2010Publication date: December 16, 2010Inventors: Pascal FURET, Frank Stephan KALTHOFF, Robert MAH, Christian RAGOT, Frédéric STAUFFER
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Publication number: 20100298141Abstract: Disclosed are compounds of Formula 1, including N-oxides, and salts thereof, wherein W is O or NR7, n is 0 or 1, and R1, R2, R3, R4, R5, R6, R7 and m are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling undesired vegetation comprising contacting the undesired vegetation or its environment with an effective amount of a compound or a composition of the invention. Also disclosed are mixtures and compositions comprising a herbicidally effective amount of a compound of Formula 1 and an effective amount of another herbicide or herbicide safener.Type: ApplicationFiled: February 8, 2008Publication date: November 25, 2010Applicant: E. I. DU PONT DE NEMOURS AND COMPANYInventors: Thomas Paul Selby, Brenton Todd Smith, Thomas Martin Stevenson
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Publication number: 20100273775Abstract: Disclosed are compounds of Formulae 1 and 1a, N-oxides, and salts thereof, wherein R1, R1a, Y, and J are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention. Further disclosed is a method for preparing compounds of Formula 1 from compounds of Formula 1a.Type: ApplicationFiled: December 10, 2008Publication date: October 28, 2010Applicant: E.I. Du pont de Nemours and CompanyInventors: John Joseph Bisaha, Alvin Donald Crews, JR., Michael Henry Howard, JR., Paula Louise Sharpe, Thomas Martin Stevenson, Andrew Edmund Taggi
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Patent number: 7790726Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally monocyclic and bicyclic compounds and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.Type: GrantFiled: August 14, 2006Date of Patent: September 7, 2010Assignee: Chemocentryx, Inc.Inventors: Penglie Zhang, Andrew M. K. Pennell, John J. Kim Wright, Lianfa Li, Edward J. Sullivan, Wei Chen, Kevin Lloyd Greenman
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Publication number: 20100210636Abstract: [PROBLEMS] To provide a compound useful as an agent for the treatment of circulatory diseases, nervous system diseases, metabolic diseases, reproductive system diseases, and digestive tract diseases. [MEANS FOR SOLVING PROBLEMS] The compound, which is for use as an active ingredient, is represented by the formula (I): [wherein R1 represents optionally halogenated C1-6 alkyl, etc.; R2 represents, e.g., a group represented by the formula (II-1) or (II-4) (wherein W represents C1-6 alkylene, etc. and R represents C1-6 alkyl, etc.); R3 represents hydrogen, C1-6 alkyl, etc.; X represents —O—, —NH—, etc.; and Y1, Y2, Y3, and Y4 each independently represents —CH—, —N—, etc.].Type: ApplicationFiled: October 2, 2008Publication date: August 19, 2010Inventors: Shiho Ishikawa, Takashi Mizutani, Tsuyoshi Nagase, Nagaaki Sato, Hidekazu Takahashi
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Publication number: 20100160304Abstract: The present invention provides a compound represented by the following formula (I): [wherein, A represents a group of the following formula (A-1): etc., R1 and R2 each independently represent a hydrogen atom etc., Z represents CR3 etc., W represents CR4 etc., Q represents CR5 etc., R3, R4 and R5 each independently represent a hydrogen atom etc., Y represents an oxygen atom or sulfur atom, X represents an oxygen atom etc. and B represents an optionally substituted aryl group or optionally substituted heteroaryl group], the prodrug thereof or the pharmaceutically acceptable salt thereof for preventing or treating various diseases such as hypertension, cerebral stroke, cardiac failure, etc.Type: ApplicationFiled: January 17, 2006Publication date: June 24, 2010Applicant: Dainippon Sumitomo Pharma Co., LtdInventor: Seiji Katayama
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Publication number: 20100099561Abstract: Disclosed are compounds of Formula 1, N-oxides, and salts thereof, wherein J is and R1, R2, R3, R4, R5, R6, R7, R8a, R8b, R8c, G1, G2, G3, G4, G5, G6, Q1, Q2, Q3, Q4, W1, W2, Y1, Y2, Y3, m and n are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling undesired vegetation comprising contacting the undesired vegetation or its environment with an effective amount of a compound or a composition of the invention.Type: ApplicationFiled: October 14, 2009Publication date: April 22, 2010Applicant: E.I. DU PONT DE NEMOURS AND COMPANYInventors: THOMAS PAUL SELBY, BRENTON TODD SMITH
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Patent number: 7666864Abstract: The current invention provides a series of bicyclic nitroimidazole-substituted phenyl oxazolidinones in which a bicyclic nitroimidazole pharmacophore is covalently bonded to a phenyl oxazolidinone, their pharmaceutical compositions, and the method of use of the compositions for prevention and treatment of bacterial infections. The bicyclic nitroimidazole-substituted phenyl oxazolidinones possess surprising antibacterial activity against wild-type and resistant strains of pathogens, and are therefore useful for the prevention, control and treatment of a number of human and veterinary bacterial infections caused by these pathogens, such as Mycobacterium tuberculosis.Type: GrantFiled: March 25, 2009Date of Patent: February 23, 2010Assignee: Global Alliance for TB Drug DevelopmentInventors: Charles Z. Ding, Genliang Lu, Keith Combrink, Dianjun D. Chen, Minsoo Song, Jiancheng Wang, Zhenkun Ma, Brian Desmond Palmer, Adrian Blaser, Andrew M. Thompson, Iveta Kmentova, Hamish Scott Sutherland, William Alexander Denny
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Patent number: 7632839Abstract: The present invention relates to fluorinated aminoalkyl-4-oxo-3,4-dihydropyrido[3,4-d]pyrimidine derivatives that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.Type: GrantFiled: January 13, 2006Date of Patent: December 15, 2009Assignee: Merck & Co. Inc.Inventors: Paul J. Coleman, George D. Hartman
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Publication number: 20090281088Abstract: The current invention provides a series of bicyclic nitroimidazole-substituted phenyl oxazolidinones in which a bicyclic nitroimidazole pharmacophore is covalently bonded to a phenyl oxazolidinone, their pharmaceutical compositions, and the method of use of the compositions for prevention and treatment of bacterial infections. The bicyclic nitroimidazole-substituted phenyl oxazolidinones possess surprising antibacterial activity against wild-type and resistant strains of pathogens, and are therefore useful for the prevention, control and treatment of a number of human and veterinary bacterial infections caused by these pathogens, such as Mycobacterium tuberculosis.Type: ApplicationFiled: March 25, 2009Publication date: November 12, 2009Applicant: Global Alliance for TB Drug DevelopmentInventors: Charles Z. Ding, Genliang Lu, Keith Combrink, Dianjun D. Chen, Minsoo Song, Jiancheng Wang, Zhenkun Ma, Brian Desmond Palmer, Adrian Blaser, Andrew M. Thompson, Iveta Kmentova, Hamish Scott Sutherland, William Alexander Denny
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Publication number: 20090181947Abstract: The present invention relates to novel bicyclic enamino(thio)carbonyl compounds, to processes for their preparation and to their use for controlling animal pests, especially arthropods, in particular insects.Type: ApplicationFiled: March 19, 2007Publication date: July 16, 2009Applicant: Bayer CropScience AGInventors: Peter Jeschke, Robert Velten, Thomas Schenke, Michael Edmund Beck, Olga Malsam, Udo Reckmann, Ralf Nauen, Ulrich Görgens, Leonardo Pitta, Christian Arnold, Erich Sanwald
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Patent number: 7547782Abstract: The present invention is directed to compounds having the formula I or II: including salts thereof, and methods for using them for the treatment of cancer.Type: GrantFiled: September 28, 2006Date of Patent: June 16, 2009Assignee: Bristol-Myers Squibb CompanyInventors: Robert M. Borzilleri, Xiao-Tao Chen, David K. Williams, John S. Tokarski, Robert F. Kaltenbach
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Publication number: 20090117440Abstract: A benzoxazine-based monomer includes a halogen atom-containing functional group and a nitrogen-containing heterocyclic group. A polymer formed from the benzoxazine-based monomer may be used in an electrode for a fuel cell and electrolyte membrane for a fuel cell.Type: ApplicationFiled: November 6, 2008Publication date: May 7, 2009Applicant: SAMSUNG ELECTRONICS CO., LTD.Inventors: Seongwoo CHOI, Jungock PARK
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Patent number: 7495096Abstract: Processes for the production of a compound of the following formula (I) by converting a compound of formula (II) with 2-pyrrolidone used in excess relative to compound (II) and processes for the production of a compound of formula (III). The latter process includes preparing compound (I); a reduction reaction which yields compound (III) in salt form; and liberating compound (III) from the salt.Type: GrantFiled: January 22, 2004Date of Patent: February 24, 2009Assignee: HF Arzneimittelforschung GmbHInventors: Joachim Moormann, Hans-Rainer Hoffmann, Rudolf Matusch
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Publication number: 20090029978Abstract: The use of a compound comprising formula (I), or a salt, ester, amide or prodrug thereof in the treatment of obesity and related disorders. The invention also relates to novel compounds within formula (I), to processes for preparing them and pharmaceutical compositions containing them. In formula (I): A is an optionally substituted thienyl moiety, Y is O, S, or NR2, R1 is a branched or unbranched alkyl (optionally interrupted by one or more oxygen atoms), alkenyl, alkynyl, cycloalkyl, cycloalkenyl, aryl, arylalkyl, reduced arylalkyl, arylalkenyl, heteroaryl, heteroarylalkyl, heteroarylalkenyl, reduced aryl, reduced heteroaryl, reduced heteroarylalkyl or a substituted derivative of any of the foregoing groups and R2 is hydrogen or a group as defined for R1.Type: ApplicationFiled: July 24, 2008Publication date: January 29, 2009Applicant: Alizyme Therapeutics LimitedInventors: Harold Francis HODSON, Christopher Robert DUNK, Richard Michael John PALMER, Dale Robert MITCHELL, Veronique BIRAULT, Russell George HUNT
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Publication number: 20080275035Abstract: The present invention relates to certain nitroimidazole compounds, which have interesting pharmaceutical properties. In particular, the compounds are useful in the treatment and/or prevention of infections such as those caused by Mycobacterium tuberculosis, Trypanosoma cruzi or Leishmania donovani. The invention also relates to pharmaceutical compositions containing the compounds, as well as processes for their preparation.Type: ApplicationFiled: December 22, 2006Publication date: November 6, 2008Inventors: Jan Jiricek, Sejal Patel, Thomas Hugo Keller, Clifton E. Barry, Cynthia S. Dowd
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Patent number: 7407954Abstract: The use of a compound comprising formula (I), or a salt, ester, amide or prodrug thereof in the treatment of obesity and related disorders. The invention also relates to novel compounds within formula (I), to processes for preparing them and pharmaceutical compositions containing them. In formula (I): A is an optionally substituted thienyl moiety, Y is O, S, or NR2, R1 is a branched or unbranched alkyl (optionally interrupted by one or more oxygen atoms), alkenyl, alkynyl, cycloalkyl, cycloalkenyl, aryl, arylalkyl, reduced arylalkyl, arylalkenyl, heteroaryl, heteroarylalkyl, heteroarylalkenyl, reduced aryl, reduced heteroaryl, reduced heteroarylalkyl or a substituted derivative of any of the foregoing groups and R2 is hydrogen or a group as defined for R1.Type: GrantFiled: August 23, 2002Date of Patent: August 5, 2008Assignee: Alizyme Therapeutics LimitedInventors: Harold Francis Hodson, Christopher Robert Dunk, Richard Michael John Palmer, Dale Robert Mitchell, Véronique Birault, Russell George Hunt
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Patent number: 7385056Abstract: An improved process for the preparation of a heteroaryl acetamide from a heteroaryl ?-hydroxyacetamide is provied. The process comprises directly hydrogenating the heteroaryl ?-hydroxyacetamide in the presence of a strong acid, a halide and a catalyst. In one embodiment, the heteroaryl acetamide is zolpidem and the heteroaryl ?-hydroxyacetamide is ?-hydroxyzolpidem.Type: GrantFiled: December 16, 2003Date of Patent: June 10, 2008Assignee: Mallinckrodt Inc.Inventors: Esa T. Jarvi, Douglas C. Miller
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Publication number: 20080125423Abstract: Compounds of the formula (I) are disclosed which are Fab I inhibitors and are useful in the treatment of bacterial infections.Type: ApplicationFiled: July 18, 2007Publication date: May 29, 2008Inventors: William H. Miller, Kenneth A. Newlander, Mark A. Seefeld, Irene N. Uzinskas, Walter E. Dewolf, Dalia R. Jakas
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Patent number: 7375103Abstract: An optically active (?)-7-[2-(cyclopropylmethoxy)-6-hydroxyphenyl]-5-[(3S)-3-piperidinyl]-1,4-dihydro-2H-pyrido[2,3-d][1,3]oxazin-2-one of the formula (I) or salt thereof.Type: GrantFiled: March 3, 2003Date of Patent: May 20, 2008Assignee: Bayer HealthCare AGInventors: Toshiki Murata, Sachiko Sakakibara, Takashi Yoshino, Hiroki Sato, Yuji Koriyama, Noriko Nunami, Megumi Yamauchi, Keiko Fukushima, Rolf Grosser, Kinji Fuchikami, Kevin Bacon, Timothy Lowinger
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Patent number: 7332498Abstract: A method of modulating KSP kinesin activity in vitro comprising contacting KSP kinesin with at least one chemical entity chosen from compounds represented by Formula I: and pharmaceutically acceptable salts thereof, where the variables are as defined further herein.Type: GrantFiled: November 23, 2005Date of Patent: February 19, 2008Assignees: Cytokinetics, Inc., SmithKline Beecham CorporationInventors: Pu-Ping Lu, David J. Morgans, Jr., Bing Yao, Dashyant Dhanak, Steven David Knight
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Patent number: 7265108Abstract: Compounds represented by the following general formula: [wherein X1, X2, X3 and X4 each independently represent a single bond, C1-6 alkylene, etc.; A2 represents optionally substituted phenyl, etc.; A1 represents an optionally substituted 5- to 7-membered heterocyclic group containing —C(=Q1)- (wherein Q1 represents oxygen, sulfur or ?N—R11 (wherein R11 represents hydrogen or C1-6 alkyl)) and nitrogen, etc.; and Z1 represents piperidin-diyl, etc.], salts thereof and hydrates of the foregoing.Type: GrantFiled: July 1, 2005Date of Patent: September 4, 2007Assignee: Eisai Co., Ltd.Inventors: Fumihiro Ozaki, Mutsuko Ono, Koki Kawano, Yoshihiko Norimine, Tatsuhiro Onogi, Takashi Yoshinaga, Kiyoaki Kobayashi, Hiroyuki Suzuki, Hiroe Minami, Kohei Sawada
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Patent number: 7259250Abstract: A C-nitroso compound having a molecular weight ranging from 225 to 1,000 (from 225 to 600 for oral administration) on a monomeric basis wherein a nitroso group is attached to a tertiary carbon, which is obtained by nitrosylation of a carbon acid having a pKa less than about 25, is useful as an NO donor. When the compound is obtained from a carbon acid with a pKa less than about 10, it provides vascular relaxing effect when used at micromolar concentrations and this activity is potentiated by glutathione to be obtained at nanomolar concentrations. When the compound is obtained from a carbon acid with a pKa ranging from about 15 to about 20, vascular relaxing effect is obtained at nanomolar concentrations without glutathione. In another embodiment, a biocompatible polymer incorporates a C-nitroso moiety.Type: GrantFiled: February 8, 2005Date of Patent: August 21, 2007Assignee: Duke UniversityInventors: Jonathan S. Stamler, Eric J. Toone
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Publication number: 20070191603Abstract: The invention is concerned with novel heterobicyclic derivatives of formula (I) wherein R1, R2, R3, R4, R5, R6, V, W, X and Y are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit L-CPT1 and can be used as medicaments.Type: ApplicationFiled: February 7, 2007Publication date: August 16, 2007Inventors: Jean Ackermann, Konrad Bleicher, Simona M. Ceccarelli, Odile Chomienne, Patrizio Mattei, Ulrike Obst Sander
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Patent number: 7189713Abstract: The present invention relates to piperidine derivatives of formula (I): R represents halogen or C1-4 alkyl R1 represents C1-4 alkyl; R2 or R3 independently represent hydrogen or C1-4 alkyl; R4 represents trifluoromethyl, C1-4 alkyl, C1-4 alkoxy, trifluoromethoxy or halogen; R5 represents hydrogen, C1-4 alkyl or C3-7 cycloalkyl; R6 is hydrogen and R7 is a radical of formula (W): ?or R6 is a radical of formula (W) and R7 is hydrogen; X represents CH2, NR5 or O; Y represents Nitrogen and Z is CH or Y represents CH and Z is Nitrogen; A represents C(O) or S(O)q, provided that when Y is nitrogen and Z is CH, A is not S(O)q; m is zero or an integer from 1 to 3; n is an integer from 1 to 3; p and q are independently an integer from 1 to 2; and pharmaceutically acceptable salts and solvates thereof. The process for their preparation and their use in the treatment of a condition mediated by tachykinins.Type: GrantFiled: February 10, 2003Date of Patent: March 13, 2007Assignee: Glaxo Group LimitedInventors: Giuseppe Alvaro, Romano Di Fabio, Maria Elvira Tranquillini, Simone Spada
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Patent number: 7112582Abstract: The present invention provides a compound of formula I, pharmaceutical compositions and the use thereof for the treatment of bacterial infection or disease in a patient in need thereof. wherein one of A and B denotes hydrogen and the other an optionally substituted fused bicyclic heteroaryl group; and X is S.Type: GrantFiled: May 1, 2003Date of Patent: September 26, 2006Assignee: WyethInventors: Aranapakam Mudumbai Venkatesan, Tarek Suhayl Mansour, Takao Abe, Itsuki Yamamura, Tsuyoshi Takasaki, Atul Agarwal, Osvaldo dos Santos, Fuk-Wah Sum, Yang-I Lin
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Patent number: 7087626Abstract: Novel pyrrazole derivative compounds and their use as pharmaceutical agents, in particular their use as TGF-beta signal transduction inhibitors.Type: GrantFiled: May 13, 2002Date of Patent: August 8, 2006Assignee: Eli Lilly and CompanyInventors: Douglas Wade Beight, Todd Vincent DeCollo, Alexander Glenn Godfrey, Theodore Goodson, Jr., Hong-Yu Li, William Thomas McMillen, Shawn Christopher Miller, Jason Scott Sawyer, Edward C. R. Smith, Jonathan Michael Yingling
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Patent number: 7064122Abstract: The subject invention features compounds having the structure: wherein X is O, S, CH2 or NR5; Y is O or S; R1 is H, substituted or unsubstituted C1-C15 alkyl, C1-C8 alkylaryl, —C(O)OR4, —C(O)NR4R5, —CR6R6?OR4, —CR6R6?OC(O)R4, —CR6R6?OC(O)NHR7, —C(O)NR10R11, —C(O)NR8R9NR8R9, —N(R5)C(O)NHR5, or CH2R4; R2 is a substituted or unsubstituted, straight chain C1—C30 alkyl or branched C3-C30 alkyl, aryl, alkylaryl, arylalkyl, heteroarylalkyl or cycloalkyl; R3 is H or substituted or unsubstituted C1-C6 alkyl or C3-C10 cycloalkyl; R4 is H or a substituted or unsubstituted, straight chain or branched, C6-C30 alkyl, aryl, —CH2-aryl, aryl —C1-C15 alkyl, heteroaryl-C1-C15alkyl or C3-C10 cycloalkyl; R5 is H or a substituted or unsubstituted, straight chain or branched, C6-C30 alkyl, aryl C1-C30alkyl, heteroarylalkyl or cycloalkyl; R6 and R6? are each independently H, substituted or unsubstituted C1-C6 alkyl, dialkyl or C3-C10 cycloalkyl or together form a 3-7 membered ring system; R7 is H or substituted or unsubstitutedType: GrantFiled: December 20, 2002Date of Patent: June 20, 2006Assignee: OSI Pharmaceuticals, Inc.Inventors: David Witter, Arlindo Castelhano
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Patent number: 7049308Abstract: A C-nitroso compound having a molecular weight ranging from 225 to 1,000 (from 225 to 600 for oral administration) on a monomeric basis wherein a nitroso group is attached to a tertiary carbon, which is obtained by nitrosylation of a carbon acid having a pKa less than about 25, is useful as an NO donor. When the compound is obtained from a carbon acid with a pKa less than about 10, it provides vascular relaxing effect when used at micromolar concentrations and this activity is potentiated by glutathione to be obtained at nanomolar concentrations. When the compound is obtained from a carbon acid with a pKa ranging from about 15 to 20, vascular relaxing effect is obtained at nanomolar concentrations without glutathione. In another embodiment, a biocompatible polymer incorporates a C-nitroso moiety.Type: GrantFiled: September 27, 2001Date of Patent: May 23, 2006Assignee: Duke UniversityInventors: Jonathan S. Stamler, Eric J. Toone
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Patent number: 6995144Abstract: The present invention provides compounds represented by the following formula: wherein X1, X2, X3 and X4 each independently represents a single bond, C1-6 alkylene, etc.; A2 represents optionally substituted phenyl, etc.; A1 represents an optionally substituted 5- to 7-membered heterocyclic group containing —C(?Q1)—, Q1 wherein represents oxygen, sulfur or ?N—R11, wherein R11 represents hydrogen or C1-6 alkyl etc.; and Z1 represents piperidin-diyl, ect, salts thereof and hydrates of the foregoing.Type: GrantFiled: March 12, 2003Date of Patent: February 7, 2006Assignee: Eisai Co., Ltd.Inventors: Fumihiro Ozaki, Mutsuko Ono, Koki Kawano, Yoshihiko Norimine, Tatsuhiro Onogi, Takashi Yoshinaga, Kiyoaki Kobayashi, Hiroyuki Suzuki, Hiroe Minami, Kohei Sawada
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Patent number: 6956034Abstract: Oxazin(ethi)one compounds of the formula I: in which the variables Z, R1, R2, R3 and n are as defined in claim 1 and A is a 5- or 6-membered carbocycle or a 5- or 6-membered heterocycle having 1, 2 or 3 heteroatoms selected from the group consisting of N, O and S, each of which cycles is attached via two carbon atoms to the oxazin(ethi)one ring, and the agriculturally useful salts of the oxazin(ethi)one compounds I are described. Moreover, the invention describes the use of compounds I and their salts for controlling phytopathogenic fungi, compositions which comprise the compounds I and/or their salts in a fungicidally effective amount and a method for controlling phytopathogenic fungi which comprises treating the fungi or the materials, plants, seeds or the soil threatened by fungal attack with a fungicidally effective amount of at least one compound of the formula I as claimed in claim 1 and/or a salt of I.Type: GrantFiled: May 17, 2002Date of Patent: October 18, 2005Assignee: BASF AktiengesellschaftInventors: Joachim Rheinheimer, Andreas Gypser, Ingo Rose, Thomas Grote, Peter Schäfer, Frank Schieweck, Eberhard Ammermann, John-Bryan Speakman, Siegfried Strathmann, Gisela Lorenz
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Patent number: 6936606Abstract: Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (Ia) and (Ib) where R1, R2, R3, R4, R5, R6, R8, R9 and X are defined herein. The compounds are useful for treating autoimmune and other diseases.Type: GrantFiled: September 27, 2002Date of Patent: August 30, 2005Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Younes Bekkali, Denice Mary Spero, Sanxing Sun, David S. Thomson, Yancey D. Ward, Erick R. R. Young, Eugene R. Hickey, Weimin Liu, Usha R. Patel
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Patent number: 6916808Abstract: The use of a compound, comprising formula (I) or a salt, ester, amide of prodrug thereof in the inhibition of an enzyme whose preferred mode of action is to catalyse the hydrolysis of an ester functionality e.g. in the control and inhibition of unwanted enzymes in products and processes. The compounds are also useful in medicine e.g. in the treatment of obesity and related conditions. The invention also relates to novel compounds within formula (I), to processes for preparing them and pharmaceutical compositions containing them.Type: GrantFiled: January 17, 2001Date of Patent: July 12, 2005Assignee: Alizyme Therapeutics LimitedInventors: Robert Downham, Richard Michael John Palmer, Harold Francis Hodson, Christopher Robert Dunk
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Publication number: 20040180838Abstract: The use of bicyclic carbohydrates for the treatment of parasite infections is described. Different bicyclic carbohydrates have been tested in vitro against a number of protozoa. These compounds also have been screened against viruses, tumors, bacteria and fungi. Compound A1, a thiophenyl-containing bicyclic carbohydrate possessed significant activity against Trypanosoma brucei rhodiense, a parasite that causes the lethal sleeping sickness. Compound A2 and Compound A3, bicyclic carbohydrates with halogen containing aryl groups, possessed significant activity against Leishmania donovani, a parasite that causes leishmaniasis. Bicyclic carbohydrates in general, and Compound A1, Compound A2 and Compound A3 more specifically, could be possible treatments for the sleeping sickness and leishmaniasis in the future.Type: ApplicationFiled: January 7, 2004Publication date: September 16, 2004Inventors: Benedikt Sas, Johan Van hemel, Jan Vandenkerckhove, Eric Peys, Johan Van der Eycken, Bart Ruttens
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Publication number: 20040181061Abstract: Oxazin(ethi)one compounds of the formula I: 1Type: ApplicationFiled: November 12, 2003Publication date: September 16, 2004Inventors: Joachim Rheinheimer, Andreas Gypser, Ingo Rose, Thomas Grote, Peter Schafer, Frank Schieweck, Eberhard Ammermann, John-Bryan Speakman, Siegfried Strathmann, Gisela Lorenz
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Patent number: 6777404Abstract: The present invention relates to compositions and methods of achieving a therapeutic effect including, the treatment or prevention of Syndrome X in an animal, preferably a mammal including a human subject or a companion animal, using a corticotropin releasing factor (CRF) antagonist alone or together with a glucocorticoid receptor antagonist.Type: GrantFiled: April 15, 2003Date of Patent: August 17, 2004Assignee: Pfizer IncInventors: Ernest S. Hamanaka, Yuhpyng Liang Chen
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Patent number: 6727258Abstract: The present invention relates to compounds of formula (IA): the preparation thereof, pharmaceutical formulations thereof, and their use in medicine as allosteric adenosine receptor modulators for uses including protection against hypoxia and ischemia induced injury and treatment of adenosine-sensitive cardiac arrhythmias.Type: GrantFiled: March 19, 2001Date of Patent: April 27, 2004Assignee: King Pharmaceutical Research & Development, Inc.Inventor: Pier Giovanni Baraldi
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Publication number: 20040053921Abstract: Disclosed are cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (Ia) and (Ib) where R2, R3, R4, R6, R8 and Y are defined herein. The compounds are useful for treating autoimmune and other diseases. Also disclosed are processes for making such novel compounds.Type: ApplicationFiled: October 24, 2002Publication date: March 18, 2004Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Younes Bekkali, Denice Mary Spero, Sanxing Sun, Yancey David Ward
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Publication number: 20040006065Abstract: The present invention relates generally to compounds that inhibit serine proteases.Type: ApplicationFiled: June 19, 2003Publication date: January 8, 2004Inventor: Peter W. Glunz
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Publication number: 20030236245Abstract: Compounds which mimic the secondary structure of helical regions of biologically active peptides and proteins having the following structure: 1Type: ApplicationFiled: August 29, 2002Publication date: December 25, 2003Applicant: Molecumetics, Ltd.Inventors: Vincent Huber, Jan Urban, Hiroshi Nakanishi, Masakatsu Eguchi, Jessymol Mathew, Min Sang Lee
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Publication number: 20030195199Abstract: The subject invention features compounds having the structure: 1Type: ApplicationFiled: December 20, 2002Publication date: October 16, 2003Inventors: David Witter, Arlindo Castelhano
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Publication number: 20030176429Abstract: The use of a compound, comprising formula (I) or a salt, ester, amide of prodrug thereof in the inhibition of an enzyme whose preferred mode of action is to catalyse the hydrolysis of an ester functionality e.g. in the control and inhibition of unwanted enzymes in products and processes. The compounds are also useful in medicine e.g. in the treatment of obesity and related conditions. The invention also relates to novel compounds within formula (I), to processes for preparing them and pharmaceutical compositions containing them. In formula (I) A is an optionally substituted 6-membered aromatic or heteroaromatic ring; and R1 is a branched or unbranched alkyl (optionally interrupted by one or more oxygen atoms), alkenyl, alkynyl, cycloalkyl, cycloalkenyl, aryl, arylalkyl, reduced arylalkyl, arylalkenyl, heteroaryl, heteroarylalkyl, heteroarylalkenyl, reduced aryl, reduced heteroaryl, reduced heteroarylalkyl or a substituted derivative of any of the foregoing groups.Type: ApplicationFiled: November 27, 2002Publication date: September 18, 2003Inventors: Robert Downham, Richard Michael John Palmer, Harold Francis Hodson, Christopher Robert Dunk
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Patent number: 6599900Abstract: The invention relates to compounds of the general formula wherein (R1)n is independently from from each other halogen, lower alkyl or lower alkoxy; R2 is hydrogen, lower alkyl, lower halogen-alkyl, —(CH2)m—OH, —(CH2)m—NR2, —(CH2)mO-lower alkyl, —(CH2)m—C(O)—NR2, or is —(CH2)m-6-membered heteroaryl, optionally substituted by one or more lower alkoxy, —(CH2)m-5 or 6-membered not aromatic heterocyclyl, optionally substituted by hydroxy or lower alkyl; R is hydrogen or lower alkyl and may be the same or different in case of R2; n is 0, 1, or 2; m is 0, 1, 2, 3 or 4; and pharmaceutically acceptable acid addition salts thereof. These compounds have a good affinity to the NK-1 receptor and they are therefore suitable for the treatment of diseases, related to this receptor.Type: GrantFiled: May 10, 2002Date of Patent: July 29, 2003Assignee: Syntex (U.S.A.) LLCInventors: Hai-Ying Cai, Michael Patrick Dillon, Guido Galley, Annick Goergler, Sabine Kolczewski, Dawn Muszynski Barsy
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Patent number: 6562811Abstract: Pyridine compounds of general formula: wherein —R1 represents in which R11 is hydrogen, C1-6 alkyl, halogen, hydroxy, C1-12 alkoxy, nitro, amino, C1-6 alkylsulfonylamino, C1-6 alkoxycarbonyl, C1-6 alkylamino, di(C1-6 alkyl)amino, C1-6 alkanoylamino, phenyl C1-6 alkylamino, phenylsulfonylamino, or —O—(CH2)n—R111; R2 represents hydrogen or halogen; R3 represents hydrogen, —CR31R32R33, or —NR34R35; R4 is hydrogen, carbamoyl, CN, carboxyl, etc.; R5 is amino, C1-6 alkylamino, di C1-6 alkylamino, etc. or salt thereof. The compound has an excellent anti-inflammatory activity, and other biological activity.Type: GrantFiled: September 18, 2001Date of Patent: May 13, 2003Assignee: Bayer AktiengesellschaftInventors: Toshiki Murata, Masaomi Umeda, Sachiko Sakakibara, Takashi Yoshino, Hiroki Sato, Tsutomu Masuda, Yuji Koriyama, Mitsuyuki Shimada, Takuya Shintani, Hiroshi Kadono, Timothy B. Lowinger, Karl B. Ziegelbauer, Kinji Fuchikami, Hiroshi Komura
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Patent number: 6559150Abstract: This invention is directed to compounds of the formula and the pharmaceutically-acceptable salts thereof, where the substituents are as defined in the specification, which are growth hormone secretogogues and which increase the level of endogenous growth hormone. The compounds of this invention are useful for the treatment and prevention of osteoporosis, congestive heart failure, frailty associated with aging, obesity; accelerating bone fracture repair, attenuating protein catabolic response after a major operation, reducing cachexia and protein loss due to chronic illness, accelerating wound healing, or accelerating the recovery of burn patients or patients having undergone major surgery; improving muscle strength, mobility, maintanence of skin thickness, metabolic homeostasis or renal homeostasis.Type: GrantFiled: November 21, 2001Date of Patent: May 6, 2003Assignee: Pfizer Inc.Inventor: Philip A. Carpino
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Patent number: 6525047Abstract: This invention is directed to compounds of the formula and the pharmaceutically-acceptable salts thereof, where the substituents are as defined in the Specification, which are growth hormone secretogogues and which increase the level of endogenous growth hormone. The compounds of this invention are useful for the treatment and prevention of osteoporosis and/or frailty, congestive heart failure, frailty associated with aging, obesity; accelerating bone fracture repair, attenuating protein catabolic response after a major operation, reducing cachexia and protein loss due to chronic illness, accelerating wound healing, or accelerating the recovery of burn patients or patients having undergone major surgery; improving muscle strength, mobility, maintenance of skin thickness, metabolic homeostasis or renal homeostasis.Type: GrantFiled: March 30, 2001Date of Patent: February 25, 2003Assignee: Pfizer Inc.Inventors: Philip Albert Carpino, David Andrew Griffith, Bruce Allen Lefker