The Additional Hetero Ring And The Bicyclo Ring System Are Attached Directly To The Same Acyclic Carbon Or Acyclic Carbon Chain Patents (Class 548/468)
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Publication number: 20100330077Abstract: Compounds of general formula (I) wherein R1 is halo or cyano; R2 is C1-C4 alkyl; and R3 is phenyl substituted with one or more substituents chosen from C1-C6 alkyl, halo or —SO2(C1-C6 alkyl); or a pharmaceutically acceptable salt, hydrate, solvate, complex or prodrug thereof; are useful in the treatment of diseases and conditions mediated by the action of PGD2 at the CRTH2 receptor.Type: ApplicationFiled: March 10, 2006Publication date: December 30, 2010Applicant: OXAGEN LIMITEDInventors: Richard Edward Armer, Edward Andrew Boyd, Philip Andrew Hay
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Publication number: 20100317709Abstract: The invention relates to compounds, in particular 2-amino-3,4,5,-trisubstituted thiophenes, pharmaceutical compositions containing them and the uses of said compounds and compositions for diseases related to sphingosine-1-phosphate (S1P) receptors, predominantly S1P3 receptors. The diseases include cardiovascular diseases, atherosclerosis, cancer, pulmonary oedema, autoimmune disorders and Adult Respiratory Distress Syndrome.Type: ApplicationFiled: November 13, 2008Publication date: December 16, 2010Inventors: Johannes Brussee, Adriaan Pieter Ijzerman, Astrid Eline Alewijnse, Stephan Leonard Maria Peters, Margot Wilhelmia Beukers
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Publication number: 20100311747Abstract: Disclosed are new dicycloazaalkane derivates represented by general formula (I), preparation processes and pharmaceutical compositions containing them, and the uses for treatment especially for dipeptidyl peptidase inhibitor (DPP-IV), in which each substitute group of general formula (I) is as defined in specification.Type: ApplicationFiled: May 20, 2008Publication date: December 9, 2010Inventors: Peng Cho Tang, Zhigang Lin, Hejun Lu, Fuqiang Zhao, Li Li, Fanglong Yang, Jianghong Fu, Lin Wang, Guangyuan Shen, Dongliang Guan
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Publication number: 20100310668Abstract: The present invention relates to a pharmaceutical composition comprising N-[2-(diethylamino)ethyl]-5-[(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide or a pharmaceutically acceptable salt thereof as active pharmaceutical ingredient.Type: ApplicationFiled: February 13, 2009Publication date: December 9, 2010Applicant: ratiopharm GmbHInventors: Jana Paetz, Frank Muskulus
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Publication number: 20100285075Abstract: The present invention relates to novel hemioxalate salt of eletriptan, process for preparation, pharmaceutical compositions, and method of treating thereof. The present invention relates to solid forms of eletriptan hemioxalate, processes for preparation, pharmaceutical compositions, and method of treating thereof. The solid form of eletriptan hemioxalate is useful for preparing eletriptan free base or a pharmaceutically acceptable salt thereof, particularly eletriptan hydrobromide, in high purity. The present invention also provides a process for preparing substantially pure eletriptan hydrobromide using eletriptan hemioxalate.Type: ApplicationFiled: December 17, 2008Publication date: November 11, 2010Applicant: ACTAVIS GROUP PTC EHFInventors: Vijaya Gopal Kusumba, Sampath Kumar Sankineni, Praveen Kumar Neela, Nitin Sharadchandra Pradhan, Jon Valgeirsson
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Patent number: 7825155Abstract: Disclosed is a compound represented by the formula (1) below, a prodrug thereof or a pharmaceutically acceptable salt of either, which is useful as a therapeutic, preventive or ameliorating agent for diabetes and the like. (In the formula, R3 represents an optionally substituted carbamoyl group or the like; X represents a hydroxyl group or the like; W1 and W2 independently represent a single bond or methylene; R7 and R8 independently represent a hydrogen atom, an optionally substituted alkyl group or the like; and Ar represents an optionally substituted aryl group or the like.Type: GrantFiled: September 13, 2006Date of Patent: November 2, 2010Assignee: Dainippon Sumitomo Pharma Co., Ltd.Inventors: Teruhisa Tokunaga, Tsuyoshi Takasaki, Kozo Yoshida, Ryu Nagata
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Publication number: 20100273724Abstract: This invention is directed to PEGlyated derivatives, drug conjugates and isotopic derivatives of certain ion channel modulating compounds.Type: ApplicationFiled: July 7, 2010Publication date: October 28, 2010Applicant: CARDIOME PHARMA CORP.Inventors: Elizabeth L. S. Cheu, Lewis Siu Leung Choi, Doug Ta Hung Chou, Allen W. Davidoff, Alan M. Ezrin, Grace Jung, Bertrand M.C. Plouvier, Aregahegn S. Yifru
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Publication number: 20100267719Abstract: Alpha-hydroxy-omega-(2-oxo-indolylidenemethyl-pyrrole-3?-carbonyl)amino alkanoic acid and amide derivatives have enhanced and unexpected drug properties as inhibitors of protein kinases and are useful in treating disorders related to abnormal protein kinase activities such as cancer.Type: ApplicationFiled: May 26, 2006Publication date: October 21, 2010Applicant: The Scripps Research InstituteInventors: Congxin Liang, Yangbo Feng, Tomas Vojkovsky
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Publication number: 20100260778Abstract: Small-molecule inhibitors of Botulinum toxin, including BoNTA, BoNTD and BoNTE are provided, as well as methods of using the inhibitors.Type: ApplicationFiled: September 20, 2006Publication date: October 14, 2010Inventors: Yuan-Ping Pang, Charles B. Millard, Jewn Giew Park, Jing Tang, James J. Schmidt
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Publication number: 20100261665Abstract: The invention relates to compounds, compositions comprising the compounds, and methods of using the compounds and compound compositions. The compounds, compositions, and methods described herein can be used for the therapeutic modulation of kinase-mediated processes, and treatment of disease and disease symptoms, particularly those mediated by certain kinase enzymes.Type: ApplicationFiled: January 28, 2010Publication date: October 14, 2010Applicant: Xcovery, Inc.Inventors: Congxin Liang, Ming Qi, Shu Gao, Zhigang Li
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Publication number: 20100256392Abstract: The present invention provides polymorphs of Sunitinib base and processes for preparation thereof.Type: ApplicationFiled: November 21, 2008Publication date: October 7, 2010Applicant: TEVA PHARMACEUTICAL INDUSTRIES LTD.Inventors: Ales Gavenda, Ettore Bigatti, Alexandr Jegorov, Augusto Canavesi, Pavel Vraspir, Judith Aronhime, Peter Lindsay MacDonald, Francesca Scarpitta, Marco Villa, Paolo Angioletti
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Publication number: 20100249129Abstract: Disclosed herein are compounds of formula (I) wherein Ring A and R1 are as defined in the specification. Pharmaceutical compositions comprising such compounds, and methods for treating conditions and disorders using such compounds and pharmaceutical compositions are also disclosed.Type: ApplicationFiled: March 26, 2010Publication date: September 30, 2010Applicant: ABBOTT LABORATORIESInventors: William A. Carroll, Michael J. Dart, Jennifer M. Frost, Steven P. Latshaw, Tongmei Li, Bo Liu, Sridhar Peddi, Xueqing Wang, Teodozyj Kolasa, Derek W. Nelson, Arturo Perez-Medrano
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Patent number: 7795250Abstract: The present invention relates to indole compounds of the formula (I): wherein R1, R2, R3, R4, A, E and X are as defined herein, and pharmaceutically acceptable salts thereof, useful in the prevention and treatment of hepatitis C infections.Type: GrantFiled: June 8, 2005Date of Patent: September 14, 2010Assignee: Istituto di Ricerche di Biologia Molecolare P Angeletti SpAInventors: Stefania Colarusso, Immacolata Conte, Joerg Habermann, Frank Narjes, Simona Ponzi
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Publication number: 20100227894Abstract: The present invention provides novel benzamide derivatives of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt, solvate, or prodrug thereof, wherein the variables A, W, Y, Z, R8, and R9 are as defined herein. These compounds are selective inhibitors of factor VIIa which can be used as medicaments.Type: ApplicationFiled: June 7, 2007Publication date: September 9, 2010Inventors: Eldon Scott Priestley, Xiaojun Zhang
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Publication number: 20100179146Abstract: Indolinone compounds of formula (I) or (II): wherein A, R1, R2, R3, R4, R5, R6, R7, and n are defined herein. Also disclosed are methods for decreasing the activity of a protein kinase and for treating a protein kinase-related disease, such as cancer, with these compounds.Type: ApplicationFiled: June 26, 2009Publication date: July 15, 2010Inventors: Jiann-Jyh Huang, Chao-Cheng Chiang, Chiawei Liu, Chun-Liang Lai, Shu Fu Lin, Yu-Hsiang Lin, Ru-Wen Wang, Sheng-Chuan Yang, Jia-Ming Chang, Shih-Hsien Chuang, Paonien Chen
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Publication number: 20100168182Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly TrkA, TrkB, TrkC, PDGFR and c-kit.Type: ApplicationFiled: December 11, 2007Publication date: July 1, 2010Applicant: IRM LLCInventors: Yuan Mi, Pamela Albaugh, Yi Fan, Ha-Soon Choi, Zuosheng Liu, Shenlin Huang
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Patent number: 7745479Abstract: The present invention relates to compounds of formula I wherein R1 to R4 and G are as defined in the description and claims and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.Type: GrantFiled: November 27, 2006Date of Patent: June 29, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Matthias Nettekoven, Jean-Marc Plancher, Hans Richter, Olivier Roche, Valerie Runtz-Schmitt, Sven Taylor
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Publication number: 20100160646Abstract: Methods for preparing sunitinib or salts thereof are described using novel intermediates and chemical pathways.Type: ApplicationFiled: March 4, 2010Publication date: June 24, 2010Applicant: TEVA PHARMACEUTICAL INDUSTRIES LTD.Inventors: Ettore Bigatti, Augusto Canavesi, Peter Lindsay Macdonald, Francesca Scarpitta
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Publication number: 20100160318Abstract: 3-pyrrolo[b]cyclohexylene-2-dihydro-indolinone derivatives of formula (I) or their pharmaceutically acceptable salts and uses thereof. The intermediates of formula (II) for preparing the above compounds. The bioassay shows that the above compounds and their pharmaceutically acceptable salts can modulate the activity of protein kinases (PKs), inhibit the activity of tyrosine kinases (PTKs) and inhibit many kinds of tumor cells as well as.Type: ApplicationFiled: December 3, 2007Publication date: June 24, 2010Applicant: JIANGSU SIMCERE PHARMACEUTICAL R&D CO., LTD.Inventors: Feng Tang, Han Shen, Qiu Jin, Lei Ding, Jie Yang, Xiaojin Yin, Shiyue Lu
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Patent number: 7741361Abstract: Compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6, and R7 are as defined herein, or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.Type: GrantFiled: December 16, 2005Date of Patent: June 22, 2010Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Daniel Kuzmich, Darren DiSalvo, John Robinson Regan, David S. Thomson
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Publication number: 20100145046Abstract: Catalysts and methods for the carbonylation of epoxides to substituted 3-hydroxy-?-lactones and ?-lactones are disclosed.Type: ApplicationFiled: November 20, 2009Publication date: June 10, 2010Inventors: Geoffrey W. Coates, John W. Kramer
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Publication number: 20100035251Abstract: The genetic polymorphism LRRK2 (leucine-rich repeat kinase 2)-T1602S is significantly associated with conversion from mild cognitive impairment (MCI) to Alzheimer's disease (AD), with the patients with TT genotype being at greater risk to progress to Alzheimer's disease. The LRRK2-T2352 also showed a trend for conversion to Alzheimer's disease, with the patients with CC genotype tending to progress to Alzheimer's disease. Similar to the APOE-E4 allele, in the presence of a BuChE-K variant, LRRK2-T1602S and LRRK2-T2352 showed a greater association with the rate of conversion from mild cognitive impairment to Alzheimer's disease. In another study with placebo-treated Alzheimer's disease patients, LRRK2-T1602S and LRRK2-T2352 showed a same trend of association. The Alzheimer's disease patients with TT genotype of LRRK2-T1602S or CC genotype of LRRK2-T2352 tended to decline faster on cognitive performance over 6 months, especially in the presence of a BuChE-K variant.Type: ApplicationFiled: June 18, 2007Publication date: February 11, 2010Inventors: Yunsheng He, Baltazar Gomez-Mancilla, Joanne Meyer, Giorgio Rovelli, Graeme Bilbe
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Publication number: 20100010234Abstract: Glutamic acid derivatives, in particular monatin, may be conveniently prepared by alkylating a 4-protected hydroxyl pyroglutamic acid derivative with an alkylating agent to prepare a 4-protected hydroxyl-4-alkylglutamic acid derivative, followed by the steps of hydrolysis and deprotection. The 4-protected hydroxyl pyroglutamic acid derivative is easy to produce from hydroxyproline. The 4-protected hydroxyl pyroglutamic acid derivative is particularly suitable for use in the efficient manufacture of monatin of high optical purity, since it can be alkylated selectively at the 4-position and stereoselectively and after its alkylation, it can easily be converted to a glutamic acid derivative.Type: ApplicationFiled: July 9, 2009Publication date: January 14, 2010Applicant: AJINOMOTO CO. INCInventor: Yusuke AMINO
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Publication number: 20090324581Abstract: To provide a novel compound which has S1P receptor agonistic activity, exhibits excellent immunosuppressing effect, gives less adverse side effects, and can be orally administered. The invention provides a compound represented by general formula (I) (wherein A is a single bond, —O—, or —CH2—; R1 represents a hydrogen atom or a C1-C6 alkyl group, and V represents any one group selected from among the following groups (1) to (3): (1) -G1-, (2) -G2-N(R2)-G3-, and (3) a group represented by formula 2, wherein each of Z1 and Z2 represents a hydrogen atom or a C1-C6 alkyl group, Z3 represents a hydrogen or the like, Q represents —CH2—O— or the like, and Y represents a group represented by formula 3, a salt thereof, or a solvate thereof.Type: ApplicationFiled: May 9, 2007Publication date: December 31, 2009Applicant: Daiichi Sankyo company LimitedInventors: Nobuo Machinaga, Toshiharu Yoshino, Jun Chiba, Jun Watanabe, Takashi Suzuki, Youichi Kimura
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Publication number: 20090318525Abstract: The invention relates to the malic acid salt of N-[2-(diethylamino)ethyl]-5-formyl-2,4-dimethyl-1H-pyrrole-3-carboxamide, to the use thereof as an intermediate for preparing the malic acid salt of sunitinib, and to pharmaceutical compositions comprising said malic acid salt of sunitinib.Type: ApplicationFiled: June 12, 2009Publication date: December 24, 2009Applicant: Medichem, S.A.Inventors: Bernardino Mangion, Stephen Benedict David Winter
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Publication number: 20090312333Abstract: The present invention concerns 2-oxo-1-pyrrolidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.Type: ApplicationFiled: May 31, 2006Publication date: December 17, 2009Applicant: UCB PHARMA, S.A.Inventors: Benoît Kenda, Yannick Quesnel, Ali Ates, Philippe Michel, Laurent Turet, Joel Mercier
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Patent number: 7629339Abstract: Alkoxy indolinone based acid and amide derivatives have enhanced and unexpected drug properties as inhibitors of protein kinases and are useful in treating disorders related to abnormal protein kinase activities such as cancer.Type: GrantFiled: September 21, 2006Date of Patent: December 8, 2009Assignee: The Scripps Research InstituteInventors: Congxin Liang, Yangbo Feng
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Publication number: 20090299077Abstract: The present invention relates to salts of (R)-5-(2-phenylsulphonylethenyl)-3-(N-methylpyrrolidin-2-ylmethyl)-1H-indole of the formula: wherein HX is an acid selected from para-toluene sulfonic acid, benzene sulphonic acid, trifluoroacetic acid, methane sulphonic acid, formic acid and succinic acid; and to processes of preparing and using such salts.Type: ApplicationFiled: May 22, 2009Publication date: December 3, 2009Inventors: Vinod Kumar KANSAL, Dhirenkumar N. MISTRY, Rakesh Ravjibhai PATEL, Saurabh PANDEY
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Publication number: 20090286973Abstract: This invention relates composition and methods for making and using chemically modified oligonucleotides agents for inhibiting gene expression.Type: ApplicationFiled: July 2, 2009Publication date: November 19, 2009Applicant: ALNYLAM PHARMACEUTICALS, INC.Inventors: Muthiah MANOHARAN, Venkitasamy KESAVAN, Kallanthottathil G. RAJEEV
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Publication number: 20090247767Abstract: Methods for preparing sunitinib or salts thereof are described using novel intermediates and chemical pathways.Type: ApplicationFiled: March 31, 2009Publication date: October 1, 2009Applicant: TEVA PHARMACEUTICAL INDUSTRIES LTD.Inventors: Ettore BIGATTI, Augusto CANAVESI, Peter Lindsay MACDONALD, Francesca Scarpitta
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Publication number: 20090227553Abstract: The present invention provides compounds of the general Formula DI: along with methods of making such compounds, formulations containing the same, and methods of using the same (e.g., in photodynamic therapy, for the production of solar cells, etc.Type: ApplicationFiled: November 30, 2006Publication date: September 10, 2009Inventors: Jonathan S. Lindsey, Joydev K. Laha, Muthiah Chinnasamy, K. Eszter Borbas
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Patent number: 7572924Abstract: The present invention relates to pyrrole substituted-2-indolinone compounds and their pharmaceutically acceptable salts which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.Type: GrantFiled: September 6, 2006Date of Patent: August 11, 2009Assignees: Sugen, Inc., Pharmacia & Upjohn Co.Inventors: Peng Cho Tang, Todd Anthony Miller, Xiaoyuan Li, Connie Li Sun, Chung Chen Wei, Shahrzad Shirazian, Congxin Liang, Tomas Vojkovsky, Asaad S. Nematalla, Michael Hawley
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Publication number: 20090186933Abstract: This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with amido piperazine derivatives. These compounds possess unique antiviral activity, whether used alone or in combination with other antivirals, antiinfectives, immunomodulators or HIV entry inhibitors. More particularly, the present invention relates to the treatment of HIV and AIDS.Type: ApplicationFiled: April 2, 2009Publication date: July 23, 2009Inventors: JOHN F. KADOW, Qiufen May Xue, Tao Wang, Zhongxing Zhang, Nicholas A. Meanwell
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Publication number: 20090182028Abstract: The present invention provides a medicament comprising a chemical compound according to formula A: wherein R1 is hydrogen, fluorine, chlorine, bromine, hydroxy, mercapto, methoxy, ethoxy, acetoxy, methyl, ethyl, propyl, isopropyl, t-butyl, nitro, amin, N,N-dimethylaminoyl, N,N-diethyl-aminoyl; R2 is hydrogen, a C1-8-alkyl e.g. methyl, ethyl, propyl, isopropyl, butyl, t-butyl; an C1-8-acyl e.g. acetyl, propionyl; R3 is a C5-12-heterocyclic ring, e.g. furanyl, pyranyl, pyrrolyl, pyridinyl, pyrazolyl, thienyl, thiazolyl, indolyl or -0R4 ; R4 is a C5-C12-aromatic ring e.g. phenyl; unsubstituted or substituted in any position with fluorine, chlorine, bromine, methoxy, ethoxy, C1-8-carboxy; Z is OH or 0; and n is 0, 1, 2 or 3, and m is 0, 1, 2 or 3, and its use for the activation of the aryl hydro carbon receptor.Type: ApplicationFiled: March 29, 2007Publication date: July 16, 2009Applicant: G.I.M. GESELLSCHAFT-FUR INNOVATIVE MEDIZIN G.M.B.H NFG OHGInventors: Alois Jungbauer, Svjetlana Medjakovic, Alfred Zöchling
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Publication number: 20090149504Abstract: The present invention relates to 5-substituted indole derivatives of formula (I): having inhibitory potential of dipeptidyl peptidase IV (DPP IV) enzyme where x and R1 are defined as defined in the specificationType: ApplicationFiled: June 15, 2006Publication date: June 11, 2009Applicant: AURIGENE DISCOVERY TECHNOLOGIES LIMITEDInventors: Venkata Subrahmanya Raja Rao Ajjarapu, Suresha Gejjalagere Puttalingaiah, Sangamesh Eshwarappa Badiger, Thomas Antony, Shekar Siddalingaiah Chelur, Syed Samiulla Dodheri, Veena Mechanda Mandappa
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Patent number: 7544698Abstract: Benzoimidazole and indole compounds are described, which are useful as H4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as allergy, asthma, autoimmune diseases, and pruritis.Type: GrantFiled: March 30, 2007Date of Patent: June 9, 2009Assignee: Janssen Pharmaceutica, N.V.Inventors: James P. Edwards, Brad M. Savall, Chandravadan R. Shah
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Publication number: 20090131398Abstract: Disclosed is a compound represented by the formula (1) below, a prodrug thereof or a pharmaceutically acceptable salt of either, which is useful as a therapeutic, preventive or ameliorating agent for diabetes and the like. (In the formula, R3 represents an optionally substituted carbamoyl group or the like; X represents a hydroxyl group or the like; W1 and W2 independently represent a single bond or methylene; R7 and R8 independently represent a hydrogen atom, an optionally substituted alkyl group or the like; and Ar represents an optionally substituted aryl group or the like.Type: ApplicationFiled: September 13, 2006Publication date: May 21, 2009Applicant: Dainippon Sumitomo Pharma Co., Ltd.Inventors: Teruhisa Tokunaga, Tsuyoshi Takasaki, Kozo Yoshida, Ryu Nagata
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Publication number: 20090124559Abstract: The invention provides compounds and methods for inhibiting proteases. One aspect of the invention features pro-soft inhibitors which react with an activating protease to release an active inhibitor moiety in proximity to a target protease. In certain instances, compounds inhibit proteasomes and/or post-proline cleaving enzymes (PPCE), such as dipeptidyl peptidase IV. The compounds of the invention provide a better therapeutic index, owing in part to reduced toxicity and/or improved specificity for the targeted protease.Type: ApplicationFiled: December 15, 2006Publication date: May 14, 2009Applicant: Trustees of Tufts College Office of Technology and Industry CollaborationInventors: William W. Bachovchin, Hung-Sen Lai, Wengen Wu
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Publication number: 20090087376Abstract: The present invention relates to the identification of compounds that are suitable for imaging amyloid deposits in living patients. The invention relates, in part, to a method of imaging amyloid deposits in brain in vivo to allow antemortem diagnosis of Alzheimer's disease. The present invention also relates to therapeutic uses for such compounds, as exemplified by compounds of the formula (1) in which Y is independently S, O, or N and m is 1, 2, or 3.Type: ApplicationFiled: July 15, 2005Publication date: April 2, 2009Applicants: The General Hospital Corporation, Massachusetts Institute of Technology, University of Pittsburg of the Commonwealth System of Higher EducationInventors: Brian Bacskai, Bradley T. Hyman, William E. Klunk, Chester A. Mathis, Timothy Swager, Evgueni Nesterov, Ivory Hills
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Publication number: 20090068718Abstract: Amino acid derivatives of pyrrolyl-indolinones and their amide or ester derivatives have enhanced and unexpected drug properties as inhibitors of protein kinases and are useful in treating disorders related to abnormal protein kinase activities such as cancer.Type: ApplicationFiled: December 28, 2006Publication date: March 12, 2009Inventors: Congxin Liang, Yangbo Feng
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Patent number: 7495111Abstract: 3-Amino chroman and 2-amino tetralin derivatives and compositions containing such compounds are disclosed. Such compounds are useful for modulating activity of a 5-HT1A receptor (agonizing or antagonizing) in a patient. These compounds are further useful for inhibiting binding to a serotonin receptor. Methods of using the 3-amino chroman and 2-amino tetralin compounds and compositions containing such compounds in the treatment of serotonin disorders, such as depression and anxiety, are also disclosed.Type: GrantFiled: June 15, 2006Date of Patent: February 24, 2009Assignee: WyethInventors: P. Sivaramakrishnan Ramamoorthy, Zhongqi Shen, Boyd L. Harrison
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Publication number: 20090048183Abstract: IAP binding molecules and compositions including these are disclosed. The IAP binding molecules interact with IAPs (inhibitor of apoptosis proteins) in cells and may be used to modify apoptosis in cells treated with such molecules. Embodiments of these compounds have a Kd of less that 0.1 micromolar. Methods of using these IAP binding molecules for therapeutic, diagnostic, and assay purposes are also disclosed.Type: ApplicationFiled: October 9, 2008Publication date: February 19, 2009Applicant: TETRALOGIC PHARMACEUTICALS CORPORATIONInventors: Stephen M. Condon, Matthew G. LaPorte, Yijun Deng, Susan R. Rippin
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Patent number: 7491744Abstract: The presently disclosed subject matter provides derivatives of non-steroidal anti-inflammatory drugs (NSAIDs) that are characterized by substantially reduced cyclooxygenase inhibiting activity, yet retain the ability to interact with and modulate the activities of other polypeptides such as the class of peroxisome proliferators-activated receptors (PPARs) and ?-secretase. Also provided are methods of using the derivatives to treat pathological disorders.Type: GrantFiled: April 26, 2005Date of Patent: February 17, 2009Assignee: Vanderbilt UniversityInventors: Lawrence J. Marnett, Jeffery J. Prusakiewicz, Andrew S. Felts, Chuan Ji
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Publication number: 20090042854Abstract: The present invention is directed to certain hexahydrpyrrolidinone compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.Type: ApplicationFiled: January 19, 2007Publication date: February 12, 2009Inventors: Jianming Bao, Robert J. DeVita, Huagang Lu, Sander G. Mills, Gregori J. Morriello
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Patent number: 7488725Abstract: Compounds are provided having the formula: wherein R1, R2, R2?, R3, R3?, R4, R4?, R5, X, Y and Z are as defined herein.Type: GrantFiled: October 30, 2006Date of Patent: February 10, 2009Assignee: Bristol-Myers Squibb Co.Inventors: Stephen P. O'Connor, Lawrence G. Hamann
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Publication number: 20080319205Abstract: The invention encompasses a process for preparing 5-bromo-3-[(R)-1-methyl-pyrrolidin-2-ylmethyl]-1H-indole comprising reacting (R)-2-(5-bromo-1H-indole-3-carbonyl)-pyrrolidine-1-carboxylic acid benzyl ester with a reducing agent selected from the group consisting of sodium dihydro-bis(2-methoxyethoxy)aluminate, lithium tris[(3-ethyl-3-pentyl)oxy]aluminohydride, lithium tri-tert-butoxyaluminum hydride and diisobutylaluminium hydride. 5-bromo-3-[(R)-1-methyl-pyrrolidin-2-ylmethyl]-1H-indole is a key intermediate for preparing eletriptan and its salts thereof.Type: ApplicationFiled: May 29, 2008Publication date: December 25, 2008Inventors: Roman Bednar, Ondrej Simo, Pavel Blatny
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Publication number: 20080317744Abstract: The present invention relates to new indole and benzimidazole compounds and pharmaceutically acceptable salts, esters or prodrugs thereof, compositions of the new compounds together with pharmaceutically acceptable carriers, and uses of the new compounds.Type: ApplicationFiled: October 14, 2005Publication date: December 25, 2008Applicant: CHIRON CORPORATIONInventors: Rustum S. Boyce, Yi Xia, Hongyan Guo, Kris G. Mendenhall, Annette O. Walter, Weibo Wang
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Publication number: 20080287519Abstract: The invention encompasses amorphous eletriptan hydrobromide, processes for preparing it and pharmaceutical compositions of it. The invention also relates to processes for preparing other forms of eletriptan hydrobromide such as Form ? and Form ?.Type: ApplicationFiled: May 1, 2008Publication date: November 20, 2008Inventors: Marioara Mendelovici, Eli Lancry, Rinat Moshkovits-Kaptsan
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Publication number: 20080275101Abstract: The present invention relates to solid salt forms of the 3-pyrrole substituted 2-indolinone compound 5-[5-fluoro-2-oxo-1,2-dihydro-indol-(3Z)-ylidenemethyl]-2,4-dimethyl-1H-pyrrole-3-carboxylic acid (2-pyrrolidin-1-yl-ethyl)-amide. It also relates to polymorphs of the phosphate salt of the amide. The invention further relates to the use of the salts and polymorphs in the treatment of protein kinase related disorders.Type: ApplicationFiled: September 8, 2006Publication date: November 6, 2008Applicants: PFIZER INC., PFIZER PRODUCTS INC.Inventors: Michael Hawley, Changquan C. Sun
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Publication number: 20080255117Abstract: The present invention relates to sulfonyltryptophanols of the general formula I, in which Q, X, W, R1, R2, R3, R4, R5, R6, R7 and R8 have the meaning as defined in the description. The compounds according to the invention are effective FSH receptor antagonists and can be used for example for fertility control in men or in women, or for the prevention and/or treatment of osteoporosis.Type: ApplicationFiled: February 29, 2008Publication date: October 16, 2008Inventors: Lars WORTMANN, Bernd Menzenbach, Marcus Koppitz, Dirk Kosemund, Hans Peter Muhn, Anna Schrey, Ronald Kuehne, Thomas Frenzel, Florian Peter Liesener