Ring Chalcogen In The Bicyclo Ring System Patents (Class 514/259.2)
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Publication number: 20100273750Abstract: The present invention relates to serotonin receptor antagonists for treating inflammatory arthritis and related conditions. The present invention also relates to a kit comprising a pharmaceutical composition comprising a serotonin receptor antagonist and instructions indicating that the composition is for use in treating inflammatory arthritis and related conditions. In addition, the present invention relates to a method of treating inflammatory arthritis and related conditions comprising administration of a serotonin receptor antagonist. The method is preferably carried out on a subject in need of treatment. The inflammatory arthritis is preferably rheumatoid arthritis.Type: ApplicationFiled: January 22, 2008Publication date: October 28, 2010Applicant: IMPERIAL INNOVATIONS LIMITEDInventors: Brian M. Foxwell, Sandra Sacre
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Publication number: 20100216819Abstract: Use of a compound of formula (I) wherein R is an alicyclic group; an arylethyl group; or phenyl or benzyl substituted by halogen, lower alkyl, alkoxy, OH, NH2, NHalkyl, N(alkyl)2, CN or NO2; in the manufacture of a medicament for the therapy of hyperalgesic pain conditions and their symptoms.Type: ApplicationFiled: June 19, 2006Publication date: August 26, 2010Inventors: Fei-Yeu Zhao, Alistair Kerr Dixon, Jonathan Mark Treherne, Chizuko Koseki, Kevin Lee, David Spanswick
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Publication number: 20100197661Abstract: The present invention provides methods for treating neurological diseases and disorders. Compounds that replace or enhance the function of SMN or alleviate or reduce a phenotype of cells with low SMN protein levels are provided. Screening methods and kits for identifying such compounds also are provided.Type: ApplicationFiled: March 23, 2010Publication date: August 5, 2010Inventors: Gideon Dreyfuss, Jin Wang
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Publication number: 20100190705Abstract: Provided herein are methods of decreasing glial fibrillary acidic protein (GFAP) levels in a cell. Such methods include administering an effective amount of a GFAP lowering compound to the cell. Also provided are compounds useful for the treatment of Alexander disease in subjects at risk of or diagnosed with Alexander disease and methods for the identification of such compounds.Type: ApplicationFiled: October 26, 2009Publication date: July 29, 2010Inventors: Albee Messing, Woosung Cho, Jon Scott Thorson, Randal D. Goff
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Publication number: 20100120745Abstract: The present disclosure relates generally to treating or preventing diseases associated with angiogenesis by administering to a patient certain compounds found to inhibit or substantially reduce angiogenesis. Compounds employed according to the present disclosure exhibit good anti-angiogenic activity as well as demonstrate a prophylactic effect for preventing and substantially reducing angiogenesis. Examples of such compounds include Ritanserin, Amiodarone, Terfenadine, Perphenazine, Bithionol, and Clomipramine.Type: ApplicationFiled: October 9, 2009Publication date: May 13, 2010Applicant: Southern Research InstituteInventors: Zhican Qu, Anshu M. Roy, Subramaniam Ananthan
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Publication number: 20100075994Abstract: The present invention relates to a series of substituted dihydro and tetrahydro oxazolopyrimidinones, specifically, to a series of 2-substituted-2,3-dihydro-oxazolo[3,2-a]pyrimidin-7-ones and 2-substituted-2,3,5,6-tetra-hydro-oxazolo[3,2-a]pyrimidin-7-ones of formula (I): Wherein p, n, X, Y, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein. This invention also relates to methods of making these compounds including novel intermediates. The compounds of this invention are modulators of metabotropic glutamate receptors (mGluR), particularly, mGluR2 receptor. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic neurodegenerative conditions, psychoses, convulsions, anxiety, depression, migraine, pain, sleep disorders and emesis.Type: ApplicationFiled: September 4, 2009Publication date: March 25, 2010Applicant: SANOFI-AVENTISInventors: Bin CAO, Vieroslava GURUNIAN, Sathapana KONGSAMUT, Raymond W. KOSLEY, JR., Rosy SHER, Ryan E. HARTUNG
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Publication number: 20090286811Abstract: The present invention provides transient receptor potential vanilloid (TRPV) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPV3. Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPV3.Type: ApplicationFiled: April 9, 2009Publication date: November 19, 2009Inventors: Prasada Rao V.S. Lingham, Sachin Sundarlal Chaudhari, Abraham Thomas, Neelima Khairatkar-Joshi, Vidya Ganapati Kattige
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Publication number: 20090176808Abstract: The present invention relates to the use of compounds and compositions of compounds having serotonin reuptake inhibiting activity and 5-HT2C antagonistic, partial agonistic or inverse agonistic activity for the treatment of depression and other affective disorders. The combined serotonin reuptake inhibiting effect and the 5-HT2C antagonistic, partial agonistic or inverse agonistic effect may reside within the same chemical compound or in two different chemical compounds.Type: ApplicationFiled: March 18, 2009Publication date: July 9, 2009Applicant: H. Lundbeck A/SInventors: Thomas Ivo Franciscus Hubert Cremers, Hakan Vilhelm Wikstrom, Johan Antonie Den Boer, Fokko Jan Bosker, Bernard Hendrik Cornelis Westerink, Klaus Peter Bogeso, Sandra Hogg, Arne Mork
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Publication number: 20090005357Abstract: The present invention relates generally to pharmacological methods for the prevention of amelioration of sleep-related breathing disorders via administration of agents or combinations of agents that possess serotonin-related pharmacological activity.Type: ApplicationFiled: September 11, 2008Publication date: January 1, 2009Applicant: THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOISInventors: Miodrag Radulovacki, David W. Carley
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Publication number: 20080242682Abstract: A combination of (S)—N-[2-(1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-yl)ethyl]propionamide with a medicine capable of prolonging a slow-wave sleep time provides a preventive or therapeutic agent for sleep disorder that induces natural sleep, shortens sleep latency, increases deep sleep, excels in sleep maintenance and ensures an appropriate sleep time.Type: ApplicationFiled: December 12, 2005Publication date: October 2, 2008Applicant: Takeda Pharmaceutical Company LimitedInventors: Keisuke Hirai, Masaomi Miyamoto
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Patent number: 7388005Abstract: The invention relates to a pyrimidone derivative represented by formula (I) or a salt thereof wherein: X represents two hydrogen atoms, a sulphur atom, an oxygen atom or a C1-2 alkyl group and a hydrogen atom; y represents a bond, an ethenylene group, an ethynylene group, an oxygen atom, a sulphur atom, a sulfonyl group, a sulfoxide group, a carbonyl group, a nitrogen atom being optionally; or a methylene group optionally substituted; R1 represents a pyrimidine group optionally substituted; R2 may represent a C1-6 alkyl group optionally substituted by a C6,10 aryloxy or a C6,10 arylamino group; a C3-6 cycloalkyl group, a C1-4 alkylthio group, a C1-4 alkoxy group, a C1-2 perhalogenated alkyl group, a C1-3 halogenated alkyl group, a phenylthio group, a benzyl group, a benzene ring, an indan ring, a 5,6,7,8-tetrahydronaphthalene ring, a naphthalene ring, a pyridine ring, a pyrrole ring, a thiophene ring, a furan ring or an imidazole ring; R3 and R4 represents each independently a hydrogen atom, C1-6 alkyl group,Type: GrantFiled: September 19, 2002Date of Patent: June 17, 2008Assignees: Sanofi-Aventis, Mitsubishi Pharma CorporationInventors: Thierry Gallet, Patrick Lardenois, Alistair Lochead, Séverine Marguerie, Alain Nedelec, Mourad Saady, Franck Slowinski, Philippe Yaiche
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Patent number: 7321033Abstract: The invention is directed to 3-?-D-ribofuranosylthiazolo[4,5-d]pyridimine nucleosides and pharmaceutical compositions containing such compounds that have immunomodulatory activity. The invention is also directed to the therapeutic or prophylactic use of such compounds and compositions, and to methods of treating diseases and disorders described herein, by administering effective amounts of such compounds.Type: GrantFiled: June 7, 2004Date of Patent: January 22, 2008Assignee: Anadys Pharmaceuticals, Inc.Inventors: Devron R. Averett, Stephen E. Webber, Joseph R. Lennox, Erik J. Rueden, David Louis Clark, Alan Xin Xiang
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Publication number: 20070281917Abstract: The invention encompasses series bicyclic pyrimidinone compounds of Formula I which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV.Type: ApplicationFiled: May 29, 2007Publication date: December 6, 2007Inventors: B. Narasimhulu Naidu, Margaret E. Sorenson
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Patent number: 7192948Abstract: The invention encompasses a series cyclic bicyclic heterocyclic compounds of Formula I which are inhibitors of HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS.Type: GrantFiled: May 26, 2005Date of Patent: March 20, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Jacques Banville, Gilles Bouthillier, B. Narasimhulu Naidu, Roger Remillard, Michael A. Walker
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Patent number: 7141564Abstract: Cyclohexane and cyclohexene derivatives and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly man.Type: GrantFiled: May 24, 2002Date of Patent: November 28, 2006Assignee: SmithKline Beecham p.l.c.Inventors: Gerald Brooks, David Thomas Davies, Graham Elgin Jones, Roger Edward Markwell, Neil David Pearson
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Patent number: 7135568Abstract: Substituted pyrazolopyrimidines and thiazolopyrimidines, specifically, compounds corresponding to the structure (I A), (I B) or (II) processes for their preparation, substance libraries containing them, pharmaceutical formulations containing these compounds, the use of these compounds for the production of medicaments for the treatment and/or prophylaxis of pain and related treatment methods are provided.Type: GrantFiled: September 12, 2003Date of Patent: November 14, 2006Assignee: Gruenenthal GmbHInventors: Matthias Gerlach, Corrinna Sundermann, Utz-Peter Jagusch, Bernd Sundermann, Martin Fuhr, Adriaan P. Ijzerman, Miriam Dissen-De Groote
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Patent number: 6900216Abstract: The present invention relates to certain novel substituted dihydroimidazo[2,1-b]thiazole and dihydro-5H-thiazolo[3,2-a]pyrimidine compounds including pharmaceutically acceptable salts thereof which have an affinity for 5-HT1A receptors and which inhibit neuronal reuptake of 5-hydroxytryptamine and/or noradrenaline, to processes for their preparation, to pharmaceutical compositions containing them and to their use in the treatment of depression, anxiety, psychoses including schizophrenia, tardive dyskinesia, obesity, drug addiction, drug abuse, cognitive disorders, Alzheimer's disease, obsessive-compulsive behaviour, panic attacks, social phobias, eating disorders such as bulimia, anorexia, snaking and binge eating, non-insulin dependent diabetes mellitus, hyperglycaemia, hyperlipidaemia, stress, as an aid to smoking cessation and in the treatment and/or prophylaxis of seizures, neurological disorders such as epilepsy and/or in which there is neurological damage such as stroke, brain trauma, cerebral ischaemiaType: GrantFiled: March 10, 2001Date of Patent: May 31, 2005Assignee: Knoll GmbHInventors: Kevin James Doyle, Frank Kerrigan, John Paul Watts
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Patent number: 6838462Abstract: The present invention relates to novel heterocyclic compounds of formula (I) where A, R1, R2, Y, Z, and n are defined in the disclosure, to processes for their preparation, and to their use as crop protection agents, in particular for controlling animal pests.Type: GrantFiled: April 16, 2002Date of Patent: January 4, 2005Assignee: Bayer CropScience LPInventors: Peter Jeschke, Michael Beck, Wolfgang Krämer, Detlef Wollweber, Angelika Lubos-Erdelen, Andreas Turberg, Olaf Hansen, Hans-Dieter Martin, Piet Sauer, Christoph Erdelen
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Publication number: 20040266765Abstract: GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women.Type: ApplicationFiled: April 13, 2004Publication date: December 30, 2004Applicant: Neurocrine Biosciences, Inc.Inventors: Joseph Pontillo, Chen Chen
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Patent number: 6833371Abstract: Compounds, compositions and methods are provided which are useful in the treatment of diseases through the inhibition of sodium ion flux through voltage-dependent sodium channels. More particularly, the invention provides pyrazolopyrimidines, compositions and methods that are useful in the treatment of central or peripheral nervous system disorders, particularly pain and chronic pain by blocking sodium channels associated with the onset or recurrance of the indicated conditions. The compounds, compositions and methods of the present invention are of particular use for treating neuropathic or inflammatory pain by the inhibition of ion flux through a channel that includes a PN3 subunit.Type: GrantFiled: November 1, 2002Date of Patent: December 21, 2004Assignee: Icagen, Inc.Inventors: Robert N. Atkinson, Michael F. Gross, Albert M. van Rhee
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Patent number: 6828326Abstract: The present invention relates to fused bicyclic metalloproteinase inhibitors of the formula wherein A, B, X, Y, and R1 are as defined in the specification, and to pharmaceutical compositions and methods of treating arthritis, inflammation, cancer and other disorders.Type: GrantFiled: August 5, 2003Date of Patent: December 7, 2004Assignee: Warner-Lambert CompanyInventors: Joseph Armand Picard, Michael William Wilson
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Publication number: 20040209896Abstract: The present application relates to novel heterocyclic compounds of formula (I) 1Type: ApplicationFiled: May 3, 2004Publication date: October 21, 2004Inventors: Peter Jeschke, Michael Beck, Wolfgang Kramer, Detlef Wollweber, Christoph Erdelen, Andreas Turberg, Olaf Hansen, Hans-Dieter Martin, Piet Sauer, Angelika Lubos-Erdelen
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Publication number: 20040209897Abstract: Compounds are described which inhibit mitogen activated protein kinase-activated protein kinase-2 (MK-2). Methods of using such compounds for the inhibition of MK-2, and for the prevention or treatment of a disease or disorder that is mediated by TNF&agr;, are described, where the method involves administering to the subject an MK-2 inhibiting compound of the present invention. Therapeutic compositions, pharmaceutical compositions and kits which contain the present MK-2 inhibiting compounds are also described.Type: ApplicationFiled: December 19, 2003Publication date: October 21, 2004Applicant: Pharmacia CorporationInventors: William F. Vernier, David R. Anderson, Dennis P. Phillion, Marvin J. Meyers, Shridhar G. Hegde, David B. Reitz, Ingrid P. Buchler, Matthew W. Mahoney, Thomas E. Rogers, Gennadiy Poda, Megh Singh, Kun K. Wu, Jin Xie
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Patent number: 6800628Abstract: This invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein R1 is C1-6alkyloxy, C2-6alkenyloxy or C2-26alkynyloxy; R2 is hydrogen or C1-6alkyloxy, or when taken together R1 and R2 may form a bivalent radical of formula wherein in said bivalent radicals one or two hydrogen atoms may be substituted with C1-6alkyl, R3 is hydrogen or halo; L is C3-6cycloalkyl, C5-6cycloalkanone, C2-6alkenyl optionally substituted with aryl, or L is a radical of formula —Alk—R4, —Alk—NR5R6, 1-R6-4-piperidinyl, Alk—X—R7, —Alk—Y—C(═O)—R9, or —Alk—Y—C(═O)—NR11R12 wherein each Alk is C1-12alkanediyl; R4 is hydrogen, C1-6alkylsulfonylamino, C3-6cycloalkyl, C5-6cycloalkanone, Ar—, di(Ar)methyl, Ar-oxy- or Het1; R5 is hydrogen or C1-6alkyl; R6 is Het2; R7 is hydrogen, C1-6alkyl, hydroxyC1-6alkyl, C3-6cycloaType: GrantFiled: November 19, 2002Date of Patent: October 5, 2004Assignee: Janssen Pharmaceutica N.V.Inventors: Jean-Paul René Marie Bosmans, Christopher John Love, Marc Gustaaf Celine Verdonck, Joannes Adrianus Jacobus Schuurkes
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Publication number: 20040127508Abstract: Substituted pyrazolopyrimidines and thiazolopyrimidines are provided along with methods for production, treatment of medical conditions and illnesses, and formulations for use as pharmaceutical compositions.Type: ApplicationFiled: September 12, 2003Publication date: July 1, 2004Inventors: Matthias Gerlach, Corrinna Maul, Utz-Peter Jagusch, Bernd Sundermann, Martin Fuhr, Adriaan P. Ijzerman, Miriam Dissen-De Groote
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Patent number: 6747032Abstract: Compound of formula (I): wherein: R1, R2, R3 and R4, which may be the same or different, each represent a hydrogen atom, a halogen atom or a group selected from alkyl, alkoxy, polyhaloalkyl, hydroxy, cyano, nitro and amino, or R1 with R2, R2 with R3, or R3 with R4, together with the carbon atoms carrying them, form an optionally substituted benzene ring or an optionally substituted heteroaromatic ring, X represents an oxygen atom or a methylene group, A represents an alkylene chain, represents an optionally substituted, unsaturated, nitrogen-containing heterocycle and R5 represents an alkyl group, its enantiomers and diastereoisomers, and addition salts thereof with a pharmaceutically acceptable acid, a medicinal products containing the same are useful as a double &agr;2/5-HT2c antagonist.Type: GrantFiled: April 18, 2002Date of Patent: June 8, 2004Assignee: Les Laboratoires ServierInventors: Gilbert Lavielle, Thierry Dubuffet, Olivier Muller, Mark Millan, Anne Dekeyne, Mauricette Brocco
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Patent number: 6740656Abstract: GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein A, R1, R2, R3a, R3b, R4, R5, R6, and n are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.Type: GrantFiled: August 2, 2002Date of Patent: May 25, 2004Assignee: Neurocrine Biosciences, Inc.Inventors: Joseph Pontillo, Chen Chen
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Patent number: 6740654Abstract: Squaric acid derivatives of formula (1) are described: wherein Het is an optionally substituted bicyclic fused ring heteroaromatic group; L2 is a covalent bond or an atom or group —O—, —S—, —C(O)—, —C(S)—, —S(O)—, —S(O)2, —N(R8)— or —C(R8)(R8a)—; Ar2 is an optionally substituted aromatic or heteroaromatic group; Alk is a chain in which R is a carboxylic acid (—CO2H) or a derivative or biostere thereof; R1 is a hydrogen atom or a C1-6alkyl group; L1 is a covalent bond or a linker atom or group; Alk1 is an optionally substituted aliphatic chain; n is zero or the integer 1; R2 is a hydrogen atom or an optionally substituted heteroaliphatic, cycloaliphatic, heterocycloaliphatic, polycycloalphatic, heteropolycycloaliphatic, aromatic or heteroaromatic group other than a 2,6-naphthyridin-1-yl, isoquinolin-1-yl, 2,7-naphthyridin-1-yl or quinazolin-4-yl group; and the saltType: GrantFiled: July 5, 2001Date of Patent: May 25, 2004Assignee: Celltech R & D LimitedInventors: Barry John Langham, Rikki Peter Alexander, John Clifford Head, Janeen Marsha Linsley, John Robert Porter, Sarah Catherine Archibald, Graham John Warrellow
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Publication number: 20040043991Abstract: The present invention relates to fused bicyclic metalloproteinase inhibitors of the formula 1Type: ApplicationFiled: August 5, 2003Publication date: March 4, 2004Inventors: Joseph Armand Picard, Michael William Wilson
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Patent number: 6696443Abstract: Certain compounds which contain a piperidine moiety flanked by aryl groups are inhibitors of p38-&agr; kinase and thus useful in the treatment of a variety of conditions characterized by inappropriate p38-&agr; kinase activity.Type: GrantFiled: November 20, 2001Date of Patent: February 24, 2004Assignee: Scios, Inc.Inventors: Babu Mavunkel, Sundeep Dugar, Gregory Luedtke, Xuefei Tan, Glenn McEnroe
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Publication number: 20040019019Abstract: The current invention discloses useful bicyclic and tricyclic amidino derivative compounds, pharmaceutical compositions containing these novel compounds, and to their use as nitric oxide synthase inhibitors.Type: ApplicationFiled: October 7, 2002Publication date: January 29, 2004Inventors: Donald W. Hansen, E. Ann Hallinan, Alok K. Awasthi, Suzanne Metz, Jeffrey A. Scholten, Jeffery S. Snyder, Mihaly V. Toth, Ronald Keith Webber
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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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Patent number: 6670365Abstract: The invention refers to new compounds of formula (I), wherein A and B are selected from the group consisting of N and CH, with the condition that when A is N, B is N; R1 is selected from the group consisting of CH3 and NH2; R2 and R3 are selected from the group consisting of H, CH3, Br, Cl, COCH3 and OCH3; and R4, R5 and R6, are selected from the group consisting of H, F, Cl, Br, (C1-C3)-alkyl, trifluoromethyl, (C1-C3)-alkoxy and trifluoromethoxy. Compounds of formula (I) are prepared by reaction of a substituted aminoazine with a substituted 2-bromo-2-(4-R1-sulfonylphenyl)-1-phenylethanone in a polar solvent. These new compounds inhibit COX-2 with high selectivity over COX-1. They are useful for the treatment of inflamation and/or cyclooxygenase-mediated diseases, having the additional advantage of a reduced potencial for ulcerogenic effects.Type: GrantFiled: April 5, 2001Date of Patent: December 30, 2003Assignee: Laboratorios S.A.L.V.A.T., S.A.Inventors: Carles Farrerons Gallemi, Ignacio-José Miquel Bono, Ana Maria Fernandez Serrat, Carlos Monserrat Vidal, Carmen Lagunas Arnal, Ferran Gimenez Guasch, Andrés Fernandez Garcia
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Publication number: 20030181456Abstract: The present invention of compounds of formula (I) 1Type: ApplicationFiled: January 29, 2003Publication date: September 25, 2003Inventors: Jean-Paul Rene Marie Andre Bosmans, Ann Louise Gabrielle Meulemans, Michel Anna Jozef De Cleyn, Henricus Jacobus Maria Gijsen
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Publication number: 20030166628Abstract: The present invention relates to certain novel substituted dihydroimidazo[2,1-b]thiazole and dihydro-5H-thiazolo[3,2-a]pyrimidine compounds of Formula (I) including pharmaceutically acceptable salts thereof in which have affinity for 5-HT1A receptors and which inhibits neuronal reuptake of 5-hydroxytryptamine and/or noradrenaline, to processes for their preparation, to pharmaceutical compositions containing them and to their use in the treatment of depression, anxiety, psychoses (for example schizophrenia), tardive dyskinesia, obesity, drug addiction, drug abuse, cognitive disorders, Alzheimer's disease, obsessive-compulsive behaviour, panic attacks, social phobias, eating disorders such as bulimia, anorexia, snacking and binge eating, non-insulin dependent diabetes mellitus, hyperglycaemia, hyperlipidaemia, stress, as an aid to smoking cessation and in the treatment and/or prophylaxis of seizures, neurological disorders such as epilepsy and/or in which there is neurological damage such asType: ApplicationFiled: January 16, 2003Publication date: September 4, 2003Inventors: Kevin James Doyle, Frank Kerrigan, John Paul Watts
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Publication number: 20030109535Abstract: GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women.Type: ApplicationFiled: August 2, 2002Publication date: June 12, 2003Applicant: Neurocrine Biosciences, Inc.Inventors: Joseph Pontillo, Chen Chen
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Publication number: 20030073704Abstract: Selected novel substituted pyrimidinone and pyridone compounds are effective for prophylaxis and treatment of diseases, such as TNF-&agr;, IL-1&bgr;, IL-6 and/or IL-8 mediated diseases, and other maladies, such as pain and diabetes. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving inflammation, pain, diabetes and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: ApplicationFiled: April 23, 2002Publication date: April 17, 2003Applicant: Amgen Inc.Inventors: Ulrike D. Spohr, Michael J. Malone, Nathan B. Mantlo, Jeffery A. Zablocki
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Publication number: 20030069231Abstract: The present invention relates to modified amino acids of general formula 1Type: ApplicationFiled: April 10, 2002Publication date: April 10, 2003Inventors: Klaus Rudolf, Wolfgang Eberlein, Wolfhard Engel, Helmut Pieper, Henri Doods, Gerhard Hallermayer, Michael Entzeroth, Wolfgang Wienen
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Publication number: 20030064962Abstract: The present invention relates generally to a novel class of pyrimidinones of Formula (I): 1Type: ApplicationFiled: December 12, 2001Publication date: April 3, 2003Inventors: Peter William Glunz, Brent Dale Douty, Wei Han
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Patent number: 6525056Abstract: Corticotropin releasing factor (CRF) antagonists of Formula (I): and their use in treating psychiatric disorders and neurological diseases, anxiety-related disorders, post-traumatic stress disorder, supranuclear palsy and feeding disorders as well as treatment of immunological, cardiovascular or heart-related diseases and colonic hypersensitivity associated with psychopathological disturbance and stress in mammals.Type: GrantFiled: February 21, 2001Date of Patent: February 25, 2003Assignee: Bristol-Myers Squibb CompanyInventors: Argyrios G. Arvanitis, Paul J. Gilligan, James P. Beck, Rajagopal Bakthavatchalam
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Publication number: 20030008885Abstract: Corticotropin releasing factor (CRF) antagonists of formula I or II: 1Type: ApplicationFiled: August 16, 2001Publication date: January 9, 2003Inventors: Liqi He, Paul Gilligan, Robert Chorvat, Argyrios Arvanitis
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Publication number: 20020077327Abstract: GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women.Type: ApplicationFiled: September 28, 2001Publication date: June 20, 2002Applicant: Neurocrine Biosciences, Inc.Inventors: Yun-Fei Zhu, Keith M. Wilcoxen, R. Scott Struthers, Chen Chen, Patrick J. Connors, Yinghong Gao, Fabio C. Tucci