1,2-diazole (including Hydrogenated) Patents (Class 546/211)
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Publication number: 20090156582Abstract: The present invention provides a pyrazole compound represented by the formula (I): wherein ring A0 is a pyrazole ring optionally further having 1 or 2 substituents; Ra is a substituted carbamoyl group; and Rb is an optionally substituted acylamino group, or a salt thereof or a prodrug thereof, which is useful as an agent for the prophylaxis or treatment of GSK-3? related pathology or disease, and a GSK-3? inhibitor including same.Type: ApplicationFiled: February 9, 2006Publication date: June 18, 2009Inventors: Tetsuya Tsukamoto, Takeshi Yamamoto, Ryosuke Tokunoh, Tomohiro Kawamoto, Masahiro Okura, Masakumi Kori, Katsuhito Murase
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Publication number: 20090149472Abstract: The present invention relates to salts of substituted pyrazoline compounds, methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animals.Type: ApplicationFiled: July 16, 2006Publication date: June 11, 2009Applicant: Laboratorios Del Dr. Esteve, S.A.Inventors: Antonio Torrens Jover, Maria Rosa Cuberes Altisen, Jose Mas Prio, Lluis Sola, Jordi Benet Buchholz
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Publication number: 20090149463Abstract: The present invention relates to compounds of formula (I) and processes for preparing such compounds, their use in the treatment of obesity, psychiatric and neurological disorders, to methods for their therapeutic use and to pharmaceutical compositions containing them.Type: ApplicationFiled: February 16, 2005Publication date: June 11, 2009Inventors: Leifeng Cheng, Eva-Lotte Lindstedt-Alstermark, Anna Maria Persdotter Boije
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Publication number: 20090137560Abstract: The present invention relates to compounds of formula (I), methods for their preparation, medicaments comprising these compounds as well their use in the manufacture of a medicament for the treatment of humans and animals.Type: ApplicationFiled: March 5, 2007Publication date: May 28, 2009Inventors: Rosa Cuberes-Altisent, Joerg Holenz
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Publication number: 20090137590Abstract: Compounds and methods are provided for the treatment of, inter alia, Type II diabetes and other diseases associated with poor glycemic control.Type: ApplicationFiled: July 10, 2008Publication date: May 28, 2009Inventors: Jingyuan Ma, Christopher J. Rabbat, Jiangao Song, Xin Chen, Imad Nashashibi, Zuchun Zhao, Aaron Novack, Dong Fang Shi, Peng Cheng, Yan Zhu, Alison Murphy
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Patent number: 7538222Abstract: Disclosed herein are compounds of Formula I, or a pharmaceutically acceptable salt, amide, ester, or prodrug thereof. Also disclosed are methods of inhibiting an activity of a monoamine receptor comprising contacting the monoamine receptor or a system containing the monoamine receptor with an effective amount of one or more of the compounds of Formula I. Disclosed are also methods of inhibiting an activation of a monoamine receptor comprising contacting the monoamine receptor or a system containing the monoamine receptor with an effective amount of one or more of the compounds of Formula I. Furthermore, methods of treating psychotic disease using a compound of Formula I are disclosed.Type: GrantFiled: December 12, 2005Date of Patent: May 26, 2009Assignee: ACADIA Pharmaceuticals, Inc.Inventors: Carl-Magnus Andersson, Nathalie Schlienger, Alma Fejzic, Eva Louise Hansen, Jan Pawlas
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Publication number: 20090124608Abstract: Compositions for the treatment of neurodegenerative diseases are disclosed. Methods of treating and monitoring progression of a neurodegenerative disease are disclosed. According to the present invention, a selective CB2 receptor modulator may be administered to a mammal for the treatment of a neurodegenerative disease.Type: ApplicationFiled: October 5, 2007Publication date: May 14, 2009Applicant: Board of Trustees of the University of ArkansasInventors: Paul L. Prather, John P. Crow
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Patent number: 7528162Abstract: The present invention relates to a group of novel 4,5-dihydro-1H-pyrazole derivatives which are potent cannabinoid (CB1) receptor antagonists with utility for the treatment of diseases connected with disorders of the cannabinoid system. The compounds have the general formula (I) wherein the symbols have the meanings given in the specification. The invention also relates to methods for the preparation of these compounds, and to pharmaceutical compositions containing one or more of these compounds as an active component.Type: GrantFiled: September 17, 2002Date of Patent: May 5, 2009Assignee: Solvay Pharmaceuticals, B.V.Inventors: Cornelis G. Kruse, Josephus H. M. Lange, Jacobus Tipker, Arnoldus H. J. Herremans, Herman H. Van Stuivenberg
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Patent number: 7524868Abstract: The present invention relates to substituted pyrazoline compounds, methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animals.Type: GrantFiled: June 27, 2005Date of Patent: April 28, 2009Assignee: Laboratorios Del Dr. Esteve, S.A.Inventors: Rosa Cuberes Altisen, Jordi Frigola Constansa, Sergio Erill Saez
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Patent number: 7524838Abstract: The present invention relates to the novel derivatives of formula (I) in which A is, if it is present, a (C1-C6) alkyl, a (C3-C6) alkenyl, a (C3-C6) alkynyl, a (C3-C7) cycloalkyl or a (C5-C7) cycloalkenyl, R1 is an NR6R7, (C4-C7) azacycloalkyl, (C5-C7) azacycloalkenyl, (C5-C9) azabicycloalkyl or (C5-C9) azabicycloalkenyl group; A-R1 is such that the nitrogen of R1 and the nitrogen in the 1-position of the pyrazole are necessarily separated by at least two carbon atoms, R3 is an H, halogen, OH, SH, NH2, ORc, SRc, SORa, SO2Ra, NHCHO, NRaRb, NHC(O)Ra, NHC(S)Ra or NHSO2Ra, R4 is an aryl or heteroaryl; and R5 is an H, halogen, CF3, CHF2, CH2F, linear or branched (C1-C6) alkyl or (C3-C7) cycloalkyl, to their racemates, enantiomers and diastereoisomers and to their mixtures, their tautomers and to their pharmaceutically acceptable salts.Type: GrantFiled: November 24, 2004Date of Patent: April 28, 2009Assignee: Aventis Pharma S.A.Inventors: Arielle Genevois-Borella, Jean-Luc Malleron, Jean Bouquerel, Gilles Doerflinger, Andrees Bohme, Gaetan Touyer, Jean-Francois Sabuco, Corrine Terrier, Serge Mignani, Michel Evers, Youssef El-Ahmad
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Patent number: 7521562Abstract: The present invention provides a filter for electronic display devices, comprising a squarylium compound represented by General Formula (I): [wherein R1 and R2 may be the same or different and each represents a hydrogen atom, an alkyl group optionally having substituent(s), an aralkyl group optionally having substituent(s), an aryl group optionally having substituent(s), or a heterocyclic group optionally having substituent(s); X represents a group represented by following Formula (A): (wherein R3 and R4 may be the same or different and represents a hydrogen atom, an alkyl group optionally having substituent(s), an alkoxy group optionally having substituent(s), an aralkyl group optionally having substituent(s), an aryl group optionally having substituent(s), or a heterocyclic group optionally having substituent(s), wherein R3 and R4 may be combined together with the adjacent nitrogen atom thereto form a heterocyclic group optionally having substituent(s))].Type: GrantFiled: July 27, 2005Date of Patent: April 21, 2009Assignee: Kyowa Hakko Chemical Co., Ltd.Inventors: Ikuo Shimizu, Junzo Yamano, Motoharu Kinugasa, Katsumi Ukai
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Patent number: 7514068Abstract: The present invention relates to biphenyl-pyrazole compounds and in particular biphenyl-pyrazolecarboxamides. The invention further provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions beneficially treated by antagonism or inverse agonism of the CB1 receptor, such as obesity, smoking cessation, and normalization of blood lipid composition.Type: GrantFiled: September 14, 2006Date of Patent: April 7, 2009Assignee: Concert Pharmaceuticals Inc.Inventor: Roger Tung
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Publication number: 20090082396Abstract: The invention is directed to 5-(hetero)aryl-4,5-dihydro-(1H)-pyrazole (pyrazoline) derivatives as cannabinoid CB1 receptor agonists, to pharmaceutical compositions comprising these compounds, to methods for their syntheses, methods for preparing novel intermediates useful for their syntheses, and methods for preparing compositions. The invention also relates to the uses of such compounds and compositions, administered to patients to achieve a therapeutic effect in disorders in which CB1 receptors are involved, or that can be treated via manipulation of those receptors. Compounds of the present invention include compounds of formula (I): wherein the substituents have the definitions given in the specification.Type: ApplicationFiled: September 19, 2008Publication date: March 26, 2009Inventors: Josephus H.M. Lange, Hicham Zilaout, Bernard J. Van Vliet
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Publication number: 20090069340Abstract: Compounds of Formula (I), wherein R1, R2, R3, R4, R5, R6, X, and n are as defined for Formula (I) in the description, processes for the preparation of the compounds and new intermediates employed in the preparation, pharmaceutical compositions containing the compounds, and the use of the compounds in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction.Type: ApplicationFiled: December 22, 2005Publication date: March 12, 2009Applicant: AstraZeneca ABInventors: Michael Balestra, Heather Bunting, Deborah Chen, Ian Egle, Janet Forst, Jennifer Frey, Methvin Isaac, Fupeng Ma, David Nugiel, Abdelmalik Slassi, Gary Steelman, Guang-Ri Sun, Babu Sundar, Radhakrishnan Ukkiramapandian, Rebecca Urbanek, Sally Walsh
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Publication number: 20090069329Abstract: The present invention provides novel pyrazoles that are useful as cannabinoid receptor antagonists and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, and/or cardiometabolic disorders.Type: ApplicationFiled: September 5, 2008Publication date: March 12, 2009Applicant: Jenrin DiscoveryInventors: John F. McElroy, Robert J. Chorvat
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Publication number: 20090048227Abstract: Substituted piperidine compounds represented by Formula I, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, sodium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, urinary incontinence, itchiness, allergic dermatitis, epilepsy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, and bipolar disorder, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds.Type: ApplicationFiled: December 18, 2006Publication date: February 19, 2009Inventors: Pasun K. Chakravarty, Pengcheng Patrick Shao, Feng Ye
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Publication number: 20090048449Abstract: The present invention relates to rimonabant monohydrate, to the process for preparing it and to the pharmaceutical compositions containing it.Type: ApplicationFiled: August 6, 2008Publication date: February 19, 2009Applicant: SANOFI-AVENTISInventors: Gerard COQUEREL, Helene DUPLAA, Baptiste FOURS, Olivier MONNIER, Philippe OCHSENBEIN
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Patent number: 7491737Abstract: The present invention is directed to compounds of the formula (I): (wherein R1, R2, R3, R4, R5, R6, R10 and n are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2.Type: GrantFiled: October 24, 2003Date of Patent: February 17, 2009Assignee: Merck & Co., Inc.Inventors: Stephen D. Goble, Alexander Pasternak, Lihu Yang
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Publication number: 20090041723Abstract: Aryl substituted pyrazole derivatives are provided, as well as processes for their preparation. The invention also provides compositions and methods for the treatment of HCV by administering a compound of the present invention, alone or in combination with additional antiviral agents, in a therapeutically effective amount.Type: ApplicationFiled: October 15, 2007Publication date: February 12, 2009Inventors: Guolin Li, Reza Fathi, Zhen Yang, Yun Liao, Qiang Zhu, Angela Man Iu Lam, Anthony Sandrasagra, Kenneth Nawoschik, Hyun-Joon Cho, Jie Cao, Wu Rouqiu, C. Richard Wobbe
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Publication number: 20090035219Abstract: Neutral antagonists of the CB1 cannabinoid receptor, means for identifying neutral antagonists of the CB1 cannabinoid receptor, and uses thereof. Antagonists of the CB1 cannabinoid receptor can be used to prevent, treat or reduce the severity of various medical conditions and symptoms, including, but not limited to obesity, appetite disorder, another metabolic disorder, drug addiction and/or mental illness. Administering neutral CB1 cannabinoid receptor antagonists in place of or in combination with known CB1 cannabinoid receptor antagonists or inverse CB1 cannabinoid receptor agonists in an individual or animal to treat a medical condition with a reduction of unwanted side effects.Type: ApplicationFiled: June 11, 2008Publication date: February 5, 2009Inventors: Alexandros Makriyannis, Venkata K. Vemuri
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Publication number: 20090029963Abstract: The invention is concerned with novel pyrazol derivatives of formula (I), wherein R1, R2, R3, R4, X and Y are as defined herein, as well as physiologically acceptable salts thereof. These compounds are antagonists of CCR-2 receptor and/or CCR-5 receptor and can be used as medicaments.Type: ApplicationFiled: July 16, 2008Publication date: January 29, 2009Inventors: Johannes Aebi, Alfred Binggeli, Luke Green, Guido Hartmann, Hans P. Maerki, Patrizio Mattei, Fabienne Ricklin, Olivier Roche
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Publication number: 20090023709Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, type II diabetes mellitus and metabolic syndrome.Type: ApplicationFiled: July 14, 2008Publication date: January 22, 2009Inventors: Paul Gillespie, Kevin Richard Guertin, Lida Qi, Qiang Zhang
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Publication number: 20090012124Abstract: The invention provides an acid addition salt of 4-(2,6-dichloro-benzoylamino)-1H-pyrazole-3-carboxylic acid piperidin-4-ylamide and crystals thereof, the salt being formed with an acid selected from methanesulphonic acid and acetic acid and mixtures thereof. Also provided are the novel uses of salts of 4-(2,6-dichloro-benzoylamino)-1H-pyrazole-3-carboxylic acid piperidin-4-ylamide, processes for the preparation of 4-(2,6-dichloro-benzoylamino)-1H-pyrazole-3-carboxylic acid piperidin-4-ylamide and its salts and novel chemical intermediates.Type: ApplicationFiled: January 20, 2006Publication date: January 8, 2009Applicant: ASTEX THERAPEUTICS LIMITEDInventors: Paul Graham Wyatt, David Charles Rees, Mladen Vinkovic, Gary Trewartha
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Publication number: 20080305041Abstract: The invention provides a novel PF4 pharmacophore that is useful, inter alia, for identifying peptidomimetics and other compounds capable of modulating PF4 activity (e.g., as inhibitors, agonists or antagonists). Mutant PF4 polypeptide sequences are also provided that modulate PF4 activity in cells.Type: ApplicationFiled: November 21, 2005Publication date: December 11, 2008Applicant: BIOQUANTA CORP.Inventors: Philippe Manivet, George Alexandre Guerin, Monica Alemany
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Publication number: 20080306068Abstract: The present invention provides kinase inhibitors of Formula I:Type: ApplicationFiled: June 15, 2005Publication date: December 11, 2008Applicant: Eli Lilly and CompanyInventors: Tiechao Li, Mark Andrew Pobanz, Chuan Shih, Yong Wang, Boyu Zhong, Jesus Andres Blas, Alfonso De Dios, Beatriz Lopez De Uralde-Garmendia, Luisa Maria Martin Cabrejas
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Publication number: 20080306069Abstract: The invention provides compounds of the formula (I), or salts, tautomers, N-oxides or solvates thereof wherein: R1 is selected from: (a) 2,6-dichlorophenyl; (b) 2,6-difluorophenyl; (c) a 2,3,6-trisubstituted phenyl group wherein the substituents for the phenyl group are selected from fluorine, chlorine, methyl and methoxy; (d) a group RO; (e) a group R a; (f) a group RIb; (g) a group RIc; (h) a group RId; and 0) 2,6-difluorophenylamino; wherein R) 0?, r R>llaa, T Rj HbD, T R) HcC, r R>Iid?, r R>>2zaa, r R>22bD and RJ are as defined in the claims. The compounds have activity as inhibitors of cdk kinase (such as cdk1 or cdk2) and glycogen synthase kinase-3 activity.Type: ApplicationFiled: January 20, 2006Publication date: December 11, 2008Applicant: ASTEX THERAPEUTICS LIMITEDInventors: Paul Graham Wyatt, Valerio Berdini, Adrian Liam Gill, Gary Trewartha, Andrew James Woodhead, Eva Figueroa Navarro, Michael Alistair O'Brien, Theresa Rachael Phillips
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Patent number: 7462632Abstract: A process for the preparation of for the preparation of N-piperidino-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methylpyrazole-3-carboxamide and of its salts, wherein 1,5-dibromopentane is reacted with a compound of formula (IIIa) in the presence of Na2CO3 in acetonitrile heated at reflux.Type: GrantFiled: November 14, 2006Date of Patent: December 9, 2008Assignee: Sanofi-AventisInventors: Philippe Vayron, Marc Daumas, Raphael Sole, Alain Dlubala
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Publication number: 20080300232Abstract: Compounds of formula I, processes for preparing such compounds, their use in the treatment of obesity, psychiatric disorders, cognitive disorders, memory disorders, schizophrenia, epilepsy, and related conditions, and neurological disorders such as dementia, multiple sclerosis, Parkinson's disease, Huntington's chorea and Alzheimer's disease and pain related disorders and to pharmaceutical compositions containing them.Type: ApplicationFiled: March 21, 2005Publication date: December 4, 2008Applicant: ASTRAZENECA ABInventors: Kay Brickmann, Bryan J. Egner, Fabrizio Giordanetto, Tord Inghardt, Anna Linusson Jonsson, Fritiof Ponten
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Publication number: 20080300278Abstract: The present invention relates to prodrugs of pyrazoline compounds of formula I, methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animals.Type: ApplicationFiled: July 17, 2006Publication date: December 4, 2008Applicant: Laboratorios Del DR. Esteve, S.A.Inventors: Antonio Torrens Jover, Susana Yenes-Minguez
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Publication number: 20080287676Abstract: The present invention discloses novel compounds of general formula (I) or a pharmaceutically acceptable salt or prodrug thereof (in which X1-X5, R5-R8b, Z1-Z2 and Ar1 are defined herein), a method for inhibiting the VR1 receptor in mammals using these compounds, a method for controlling pain in mammals, and pharmaceutical compositions including those compounds and a process for making those compounds.Type: ApplicationFiled: April 30, 2008Publication date: November 20, 2008Applicant: Abbott LaboratoriesInventors: Arthur R. Gomtsyan, Erol K. Bayburt, Chih-Hung Lee, John R. Koenig, Robert G. Schmidt, Kirill A. Lukin, Gilles Chambournier, Margaret Chi-Ping Hsu, Robert M. Leanna, Russell D. Cink
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Patent number: 7452907Abstract: Compounds are provided which have the structure wherein Q is C or N, X1 is C or N, and R1, R2, R2a, R2b, R2c, R3, Y, A, m, n, X2, X3 and X4 are as defined herein, which compounds are useful as antidiabetic, hypolipidemic, and antiobesity agents.Type: GrantFiled: April 19, 2006Date of Patent: November 18, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Peter T. Cheng, Yoon Jeon, Wei Wang
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Publication number: 20080280925Abstract: The present invention relates to compounds that are useful as inhibitors of protein arginine methyltransferase that have a formula selected from Formula (I), Formula (II) and Formula (III), as well as racemic mixtures, diastereomers, enantiomers and tautomers thereof and N-oxides, hydrates, solvates, pharmaceutically acceptable salts, prodrugs and complexes thereof as defined herein. Said compound are useful as inhibitors of PRMTs and/or CARM-I. The invention further relates to compositions comprising such compounds and methods for their use.Type: ApplicationFiled: February 28, 2008Publication date: November 13, 2008Inventors: Amal Wahhab, Eric Therrien, Martin Allan, Sukhdev Manku
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Publication number: 20080269294Abstract: The invention concerns benzamide compounds of formula (I), wherein R1 is a C-linked pyrazole ring, which is optionally substituted by one or more groups selected from C1-4alkyl, C3-4cycloalkyl, C1-4alkoxy and C3-4cycloalkoxy; or a pharmaceutically acceptable salt or pro-drug form thereof. The invention also concerns processes for the preparation of such compounds, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumours or other proliferative conditions, which are sensitive to the inhibition of histone deacetylase (HDAC).Type: ApplicationFiled: October 17, 2005Publication date: October 30, 2008Applicant: ASTRAZENECA ABInventors: David Michael Andrews, Elaine Sophie Elizabeth Stokes, Andrew Turner, Michael James Waring
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Publication number: 20080269207Abstract: The invention provides compounds of the formula (0) or salts or tautomers or N-oxides or solvates thereof for use in the prophylaxis or treatment of disease states and conditions such as cancers mediated by cyclin-dependent kinase and glycogen synthase kinase-3. In formula (0): X is a group R1-A-NR4— or a 5- or 6-membered carbocyclic or heterocyclic ring; A is a bond, SO2, C?O, NRg(C?O) or O(C?O) wherein Rg is hydrogen or C1-4 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy; Y is a bond or an alkylene chain of 1, 2 or 3 carbon atoms in length; R1 is hydrogen; a carbocyclic or heterocyclic group having from 3 to 12 ring members; or a C1-8 hydrocarbyl group optionally substituted by one or more substituents selected from halogen (e.g.Type: ApplicationFiled: October 19, 2007Publication date: October 30, 2008Applicant: ASTEX THERAPEUTICS, LTD.Inventors: Valerio Berdini, Michael Alistair O'Brien, Maria Grazia Carr, Theresa Rachel Early, Adrian Liam Gill, Gary Trewartha, Alison Jo-Anne Woolford, Andrew James Woodhead, Paul Graham Wyatt
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Publication number: 20080269293Abstract: This invention relates to novel compounds of formula (I) or stereoisomers or pharmaceutically acceptable salts thereof wherein Y, R1 through R9, and X1 through X7 are as defined in the specification, pharmaceutical compositions containing said compounds useful as P2Y1 antagonists, and to methods of treating thromboembolic disorders.Type: ApplicationFiled: August 22, 2007Publication date: October 30, 2008Inventors: Liguo Chi, Chulho Choi, Andrew G. Geyer, Robert M. Kennedy, Jeffery A. Pfefferkorn, Roy T. Winters
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Patent number: 7432379Abstract: Disclosed are compounds that are bradykinin B1 receptor antagonists and are useful for treating diseases, or relieving adverse symptoms associated with disease conditions, in mammals mediated by bradykinin B1 receptor. Certain of the compounds exhibit increased potency and are also expected to exhibit increased duration of action.Type: GrantFiled: April 30, 2004Date of Patent: October 7, 2008Assignee: Elan Pharmaceuticals, Inc.Inventors: Jay S. Tung, Albert W. Garofalo, Michael A. Pleiss, Jing Wu, David W. G. Wone, Ashley C. Guinn, Darren B. Dressen, R. Jeffrey Neitz, Jennifer Marugg, Martin Neitzel
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Patent number: 7429581Abstract: The present invention is directed to a compound of formula I, in which R0; R1; R2; R3; R4; Q; V, G and M have the meanings indicated below. The compound of formula I is a pharmacologically active compound. It exhibits a strong anti-thrombotic effect and is suitable, for example, for the therapy and prophylaxis of a cardio-vascular disorder like a thromboembolic disease or restenosis. It is a reversible inhibitor of the blood clotting enzymes factor Xa (FXa) and/or factor VIIa (FVIIa), and can in general be applied in conditions in which an undesired activity of factor Xa and/or factor VIIa is present or for the cure or prevention of which an inhibition of factor Xa and/or factor VIIa is intended. The invention furthermore is directed to a process for the preparation of the compound of formula I, and pharmaceutical preparation comprising it.Type: GrantFiled: December 23, 2003Date of Patent: September 30, 2008Assignee: Sanofi-Aventis Deutschland GmbHInventors: Marc Nazare, Volkmar Wehner, David W. Will, Hans Matter
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Publication number: 20080234323Abstract: The present invention describes novel forms of Rimonabant hydrochloride, processes for their preparation and pharmaceutical compositions containing them. Thus, the present invention discloses three new crystalline forms designated as Form II, Form III and Form IV of Rimonabant hydrochloride and novel amorphous forms of the salt.Type: ApplicationFiled: January 6, 2006Publication date: September 25, 2008Inventors: Braj Bhushan Lohray, Vidya Bhushan Lohray, Bipin Pandey, Mayank Ghanshyambhai Dave, Parind Narendra Dholakia
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Patent number: 7423052Abstract: A invention relates to N aroyl cyclic amine derivatives and their use as pharmaceuticals, specifically as orexin receptor antagonists.Type: GrantFiled: June 25, 2002Date of Patent: September 9, 2008Assignee: SmithKline Beecham p.l.c.Inventors: Wai Ngor Chan, Amanda Johns, Christopher Norbert Johnson, Riccardo Novelli, Roderick Alan Porter
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Publication number: 20080207637Abstract: The present invention relates to substituted pyrazoline compounds, methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animal.Type: ApplicationFiled: February 14, 2005Publication date: August 28, 2008Inventors: Rosa Cuberes Altisen, Bonifacio Gutierrez Silva, Jordi Frigola- Constansa
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Publication number: 20080194562Abstract: The invention provides compounds of the formula (I) or a salt, tautomer, solvate or N-oxides thereof; wherein: R1 is selected from (a) 2,6-dichlorophenyl; (b) 2,6-difluorophenyl; (c) a 2,3,6-trisubstituted phenyl group wherein the substituents are fluorine, chlorine, methyl or methoxy; and (d) a group R0 wherein R0 is a 3-12 membered carbocyclic or heterocyclic group; or optionally substituted C1-8 hydrocarbyl; R2a and R2b are each hydrogen or methyl; and R3 is as defined in the claims. The compounds have activity as inhibitors of Cyclin Dependent Kinases (CDK) and Glycogen Synthase Kinases (GSK) kinases and are useful in the treatment or prophylaxis of disease states or conditions mediated by the kinases.Type: ApplicationFiled: January 20, 2006Publication date: August 14, 2008Applicant: ASTEX THERAPEUTICS LIMITEDInventors: Paul Graham Wyatt, Valerio Berdini, Adrian Liam Gill, Gary Trewartha, Andrew James Woodhead, Eva Figueroa Navarro, Michael Alistair O'Brien, Theresa Rachael Phillips
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Patent number: 7407972Abstract: The present invention provides compounds of Formula (I): wherein A, B, C, G, and W1 have any of the values defined in the specification, and pharmaceutically acceptable salt thereof, that are useful to treat thrombotic disorders. Also disclosed are pharmaceutical compositions comprising one or more compounds of Formula I, processes for preparing compounds of Formula I, and intermediates useful for preparing compounds of Formula I.Type: GrantFiled: December 20, 2004Date of Patent: August 5, 2008Assignee: Pfizer Inc.Inventor: Jeremy John Edmunds
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Publication number: 20080182837Abstract: The present invention encompasses compounds of general formula (1) wherein the groups R2 to R4, L, Q and n are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.Type: ApplicationFiled: July 5, 2007Publication date: July 31, 2008Inventors: Steffen STEURER, Peter Ettmayer, Andreas Mantoulidis, loannis Sapountzis, Martin Steegmaier
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Publication number: 20080182877Abstract: Various solid state forms of rimonabant have been found, including a particulate amorphous form as well as several hydrates and solvates.Type: ApplicationFiled: December 21, 2007Publication date: July 31, 2008Inventor: Raymond J.H. Westheim
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Patent number: 7396929Abstract: This application discloses a novel process to synthesize 3-amino-4-substituted pyrazole derivatives, which may be used, for example, as intermediates to prepare compounds having, for example, pharmaceutical utility.Type: GrantFiled: June 7, 2006Date of Patent: July 8, 2008Assignee: Schering CorporationInventors: Jianshe Kong, Tao Meng, Paul E. McNamara, Xian Liang, Jesse K. Wong
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Patent number: 7393842Abstract: One aspect of the invention is concerned with cannabimimetic pyrazole analogs. Another aspect of the invention is concerned with new and improved pyrazole analogs having high affinities and/or selectivities for the CB1 cannabinoid receptor. A further aspect of the invention is concerned with pharmaceutical preparations employing the inventive analogs and methods of administering therapeutically effective amounts of the inventive analogs to provide a physiological effect.Type: GrantFiled: March 1, 2004Date of Patent: July 1, 2008Assignee: University of ConnecticutInventors: Alexandros Makriyannis, Qian Liu, Rajesh Thotapally
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Publication number: 20080153812Abstract: There is provided a compound of formula (I): or a pharmaceutically acceptable salt thereof. There are also provided processes for the manufacture of a compound of Formula 1, and the use of a compound of Formula 1 as a medicament and in the treatment of cancer.Type: ApplicationFiled: December 18, 2007Publication date: June 26, 2008Applicant: ASTRAZENECA ABInventors: David Buttar, Kevin Micheal Foote, Maria-Elena Theoclitou, Andrew Peter Thomas
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Publication number: 20080153810Abstract: The present invention relates to novel compounds, in particular, novel indazole that may be used as melanin concentrating hormone receptor ligands, methods of preparing such compounds, compositions containing such compounds, and methods of using such compounds to treat MCH related disorders.Type: ApplicationFiled: November 14, 2007Publication date: June 26, 2008Applicant: Forest Laboratories Holdings LimitedInventors: Matthew Ronsheim, Gian-Luca Araldi
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Publication number: 20080146614Abstract: The present invention relates to 1,5-diphenylpyrazole compounds of formula I (A chemical formula should be inserted here—please see paper copy enclosed herewith) and processes for preparing such compounds, their use in the treatment of obesity, psychiatric and neurological disorders, to methods for their therapeutic use and to pharmaceutical compositions containing them.Type: ApplicationFiled: December 21, 2005Publication date: June 19, 2008Inventor: Leifeng Cheng
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Publication number: 20080139621Abstract: The invention relates to compounds and their use in the treatment of thrombocytopenia resulting from diseases or conditions such as immune thrombocytopenic purpura, cancer chemotherapy, surgery, bone marrow or stem cell transplantation, radiation injury or treatment, chronic viral infection, and pancytopenia. The invention further relates to pharmaceutical compositions containing the compounds and compositions of the invention as well as methods for treating such diseases or conditions in a mammal, including a human, by administering to such mammal an effective amount of a selected thrombopoietin receptor agonist.Type: ApplicationFiled: November 30, 2007Publication date: June 12, 2008Applicant: STATegics, Inc.Inventors: Jeffrey R. Spencer, Juha Punnonen