The Five-membered Hetero Ring Is One Of The Cyclos In A Bicyclo Ring System Patents (Class 544/373)
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Publication number: 20100292187Abstract: The present invention provides compounds, pharmaceutical compositions, and methods of using such compounds or compositions for treating infection by a virus, or for affecting viral IRES activity.Type: ApplicationFiled: June 14, 2010Publication date: November 18, 2010Applicant: PTC THERAPEUTICS, INC.Inventors: Gary M. Karp, Peter Seongwoo Hwang, James J. Takasugi, Hongyu Ren, Richard Gerald Wilde, Anthony A. Turpoff, Alexander Arefolov, Guangming Chen, Jeffrey A. Campbell, Chunshi Li, Steven Paget, Nanjing Zhang, Xiaoyan Zhang, Jin Zhu
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Publication number: 20100292219Abstract: The present invention provides tertiary amine substituted peptides of Formula (I) useful as inhibitors of HCV replication. The variables R and R1-R12 in Formula I are described herein. The invention also includes methods for preparing such compounds. The present invention further includes pharmaceutical compositions containing tertiary amine substituted peptides and methods for using such compounds, including methods for using the compounds to treat hepatitis C infection.Type: ApplicationFiled: February 26, 2008Publication date: November 18, 2010Applicant: ACHILLION PHARMACEUTICALS, INC.Inventors: Atul Agarwal, Xiangzhu Wang, Dawei Chen, Suoming Zhang, Avinash Phadke
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Patent number: 7834004Abstract: Compounds as modulators of peroxisome proliferator activated receptors, pharmaceutical compositions comprising the same, and methods of treating disease using the same are disclosed.Type: GrantFiled: September 4, 2008Date of Patent: November 16, 2010Assignee: Kalypsys, IncInventors: Stewart A. Noble, Guy Oshiro, James W. Malecha, Cunxiang Zhao, Carmen Robinson, Sergio G. Duron, Michael Sertic, Andrew K. Lindstrom, Andrew K. Shiau, Christopher D Bayne, Mehmet Kahraman, Boliang Lou, Steven P. Govek
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Patent number: 7834020Abstract: The invention relates to new crystalline modifications of the hydrochloride of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine, crystalline modification of the dihydrochloride of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine and amorphous 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride which are suitable in particular for the preparation of solid medicaments for the treatment or prevention of depressive disorders, anxiety disorders, bipolar disorders, mania, dementia, substance-related disorders, sexual dysfunctions, eating disorders, obesity, fibromyalgia, sleeping disorders, psychiatric disorders, cerebral infarct, tension, for the therapy of side-effects in the treatment of hypogonadism, secondary amenorrhea, premenstrual syndrome and undesired puerperal lactation.Type: GrantFiled: April 28, 2008Date of Patent: November 16, 2010Assignee: Merck Patent GesellschaftInventors: Andreas Bathe, Bernd Helfert, Steffen Neuenfeld, Heike Kniel, Matthias Bartels, Susanne Rudolph, Henning Böttcher
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Publication number: 20100285515Abstract: A compound represented by the following general formula (I): [wherein R1 and R2 represent a C1-6 alkyl group; R3, R4 and R5 represent hydrogen atom, a C1-6 alkyl group, or an aryl group; Y1 and Y2 represent —O—, —S—, —Se—, —CH?CH—, —C(R6)(R7)—, or —N(R8)— (wherein R6, R7 and R8 represent hydrogen atom or a C1-6 alkyl group); A represents a C1-3 alkylene group; n and n? represent 0, 1 or 2; Z1 and Z2 represent a nonmetallic atom group required to form a benzo-condensed ring or a naphtho-condensed ring; L1 to L7 represent a methine group; and M? represents a counter ion in a number required for neutralizing electrical charge], which is useful as a fluorescent probe of which optical characteristics change depending on pH change.Type: ApplicationFiled: February 15, 2008Publication date: November 11, 2010Applicant: THE UNIVERSITY OF TOKYOInventors: Tetsuo Nagano, Hirotatsu Kojima, Kazuki Kiyose
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Patent number: 7829713Abstract: The invention includes a compound of formula I: wherein R1, X, Z, n, and m have any of the values described herein, as well as salts of such compounds, compositions comprising such compounds, and therapeutic methods that comprise the administration of such compounds. The compounds are inhibitors of PDE4 function and are useful for improving cognitive function in animals.Type: GrantFiled: February 27, 2007Date of Patent: November 9, 2010Assignee: Helicon Therapeutics, Inc.Inventors: Terrence P. Keenan, Alan P. Kaplan
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Publication number: 20100280012Abstract: An azaazulene compound is provided. The azaazulene compound has formula (I) shown below. Each variable in formula (I) is defined in the specification. The compound can be used to treat cancer. The invention also provides a method for treating cancer. The method includes administering to a subject in need thereof an effective amount of one or more azaazulene compounds of formula (I).Type: ApplicationFiled: April 28, 2010Publication date: November 4, 2010Applicant: INDUSTRIAL TECHNOLOGY RESEARCH INSTITUTEInventor: On LEE
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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: 20100273774Abstract: A compound of formula (I), wherein R, R1, R2, ring A, which ring contains one or two nitrogen atoms, and ring B are as defined in the Specification, pharmaceutical compositions containing these compounds, and uses for these compounds and compositions, in particular, in transplantation.Type: ApplicationFiled: July 9, 2010Publication date: October 28, 2010Inventors: Jürgen Wagner, Maurice Van Eis, Peter Von Matt, Jean-Pierre Evenou, Walter Schuler
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Patent number: 7816376Abstract: The invention relates to compounds of the formula (I) and pharmaceutically usable derivatives, salts, solvates and stereoisomers and mixtures thereof, in which X, Y, Z, R1, R3, R4, R8, p, k, E, G, Z and Q are as defined in claim 1, which are employed as excitatory amino acid antagonists for combating neurodegenerative diseases, including cerebrovascular diseases, epilepsy, schizophrenia, Alzheimer's, Parkinson's or Huntington's disease, cerebral ischaemia, infarction or psychoses.Type: GrantFiled: March 5, 2003Date of Patent: October 19, 2010Assignee: Merck Patent GmbHInventors: Oliver Schadt, Joachim Leibrock, Helmut Pruecher, Christoph Seyfried
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Patent number: 7807678Abstract: The invention relates to a method of deriving a peptidomimetic of a biologically active metallopeptide, wherein the peptidomimetic includes at least one non-peptide ring structure defining a template space superimposable on a corresponding defined template space of the metallopeptide, and where the peptidomimetic further includes at least two elements independently including an amino acid residue, amino acid side chain moiety or derivative thereof, the elements defining and occupying a similar descriptor space as corresponding elements of the metallopeptide. The invention further relates to peptidomimetics with a template space heterocyclic ring structure, including 5-, 6- and 8-membered and 5-5- and 6-5-bicyclic fused ring structure melanocortin receptor-specific peptidomimetics.Type: GrantFiled: February 10, 2004Date of Patent: October 5, 2010Assignee: Palatin Technologies, Inc.Inventors: Shubh D. Sharma, Yi-Qun Shi, Zhijun Wu, Ramesh Rajpurohit
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Patent number: 7803803Abstract: The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts thereof, wherein: X is CH or N; one of R1 and R2 is H, and the other is selected from OR6, SR6, NR6R7, N3, Me, Et, CF3, SOR8 and SO2R8; R3 is selected from tert-butylmethyl, iso-propylmethyl, sec-butyl, tert-butyl, cyclopentyl and cyclohexyl; R4 is optionally substituted C1-8 alkyl or optionally substituted C3-8 cycloalkyl; R6 and R7 are each independently selected from H, C1-8-alkyl and C3-8-cycloalkyl, or R6 and R7 are linked to form a cyclic group together with the nitrogen to which they are attached; and R8 is C1-8-alkyl or C3-8-cycloalkyl.Type: GrantFiled: January 8, 2009Date of Patent: September 28, 2010Assignee: Amura Therapeutics LimitedInventors: Martin Quibell, John Paul Watts
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Publication number: 20100240642Abstract: The present invention relates to certain indole derivatives that are modulators of PPAR?, to processes for their preparation, to pharmaceutical compositions containing them and to their use in medicine.Type: ApplicationFiled: August 31, 2007Publication date: September 23, 2010Applicant: SMITHKLINE BEECHAM CORPORATIONInventors: Jeffrey Alan Oplinger, Paul Kenneth Spearing, Millard Hurst Lambert, John A. Ray, Christopher P. Laudeman, Jerzy R. Szewczyk, Pierette Banker
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Publication number: 20100240650Abstract: The present invention is directed to novel substituted pyrroline compounds useful as kinase or dual-kinase inhibitors, methods for producing such compounds and methods for treating or ameliorating a kinase or dual-kinase mediated disorder.Type: ApplicationFiled: May 25, 2010Publication date: September 23, 2010Inventors: Han-Cheng Zhang, Bruce E. Maryanoff, David F. McComsey, Kimberly White, Hong Ye, Leonard R. Hecker, Bruce Conway, Keith Demarest
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Patent number: 7799916Abstract: The invention relates to a process for the preparation of 5-(4-[4-(5-cyano-3-indolyl)butyl]-1-piperazinyl)benzofuran-2-carboxamide and/or one of its physiologically acceptable salts, characterized in that a compound of the formula (I), in which L denotes Cl, Br, I, SO2F, SO2CF3, SO2C2F5, is reacted with 3-(4-piperazin-1-ylbuyl)indole-5-carbonitrile by transition-metal-catalyzed coupling by means of Pd complexes, and/or in that the 5-(4[4-(5-cyano-3-indolyl)butyl]-1-piperazinyl)benzofuran-2-carboxamide formed is converted into one of its acid-addition salts by treatment with an acid, and to a second process, characterized in that a compound of the formula (II), as the base or HX salt (where X=Cl, BR), is reacted with 3-(4-oxobutyl)-1H-indole-5-carbonitrile by reductive amination, and/or in that 5-(4-[4-(5-cyano-3-indolyl)butyl]-1-piperazinyl)benzofuran-2-carboxamide is converted into one of its acid-addition salts by treatment with an acid.Type: GrantFiled: April 12, 2006Date of Patent: September 21, 2010Assignee: Merck Patent GmbHInventor: Andreas Bathe
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Patent number: 7799791Abstract: A compound of formula (I), or a pharmaceutically acceptable salt, hydrate, complex or pro-drug thereof, wherein: one of R1 and R2 is H, and the other is selected from OR6, SR6, NR6R7, N3, Me, Et, CF3, SOR8 and SO2R8; or R1 and R2 are both H; one of R3 and R4 is H, and the other is selected from tert-butylmethyl, iso-propylmethyl, sec-butyl, tert-butyl, cyclopentyl and cyclohexyl; or R3 and R4 are joined together with the adjacent backbone carbon atom to form a spiro-C5-C6 cycloalkyl group; R6 and R7 are each independently selected from H, C1-8-alkyl and C3-8-cycloalkyl; or R6 and R7 are linked to form a cyclic group together with the nitrogen to which they are attached; R8 is C1-8-alkyl or C3-8-cycloalkyl; R9 is a para-substituted 6-membered monocyclic aryl or heteroaryl ring which includes up to five heteroatoms.Type: GrantFiled: January 8, 2009Date of Patent: September 21, 2010Assignee: Amura Therapeutics LimitedInventors: Martin Quibell, John Paul Watts
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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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Patent number: 7795266Abstract: Compositions comprising tetrahydroindolone derivatives in which the tetrahydroindolone moiety is covalently linked to a substituted arylpiperazine moiety and methods for treating neurological and psychiatric conditions using such compositions are disclosed.Type: GrantFiled: September 27, 2004Date of Patent: September 14, 2010Inventors: David R. Helton, David B. Fick, Jason P. Sharp, Ernest H. Pfadenhauer
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Publication number: 20100226918Abstract: The present invention relates to compounds of the formula I, in which R1; R2; R3; R4; R5; R6; R7; R8; R9; R10; R11; R12; R13; A; B, D and E have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong anti-aggregating effect on platelets and thus an anti-thrombotic effect and are suitable e.g. for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are reversible antagonists of the platelet ADP receptor P2Y12, and can in general be applied in conditions in which an undesired activation of the platelet ADP receptor P2Y12 is present or for the cure or prevention of which an inhibition of the platelet ADP receptor P2Y12 is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.Type: ApplicationFiled: December 16, 2009Publication date: September 9, 2010Applicant: SANOFI-AVENTISInventors: Otmar KLINGLER, Joerg CZECH, Werngard CZECHTIZKY, Tilo WEISS, Melitta JUST
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Patent number: 7790726Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally monocyclic and bicyclic compounds and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.Type: GrantFiled: August 14, 2006Date of Patent: September 7, 2010Assignee: Chemocentryx, Inc.Inventors: Penglie Zhang, Andrew M. K. Pennell, John J. Kim Wright, Lianfa Li, Edward J. Sullivan, Wei Chen, Kevin Lloyd Greenman
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Publication number: 20100222363Abstract: New bicyclic derivatives of formula (I); wherein the meanings for the various substituents are as disclosed in the description. These compounds are useful as p38 kinase inhibitors.Type: ApplicationFiled: June 28, 2006Publication date: September 2, 2010Applicant: PALAU PHARMA, S.A.Inventors: Carmen Almansa Rosales, Marina Virgili Bernadó
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Publication number: 20100222358Abstract: Octahydro-pyrrolo[3,4-b]pyrrole derivatives are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Octahydro-pyrrolo[3,4-b]pyrrole compounds, methods for using such compounds, compositions for making them, and processes for preparing such compounds are disclosed herein.Type: ApplicationFiled: March 2, 2010Publication date: September 2, 2010Applicant: ABBOTT LABORATORIESInventors: Marlon D. Cowart, Chen Zhao, Minghua Sun, Lawrence A. Black, Guo Zhu Zheng, Robert J. Gregg, Geoff G.Z. Zhang, Ahmad Y. Sheikh, Xiaochun Lou, Rodger F. Henry, David M. Barnes, Lawrence Kolaczkowski, Anthony R. Haight, Sou-Jen Chang, Steven J. Wittenberger, Michael G. Fickes
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Publication number: 20100222322Abstract: Indole compounds of Formula (I) are HIV reverse transcriptase inhibitors, wherein R1, R2, R3, R4 and R5 are defined herein. The compounds of Formula (I) and their pharmaceutically acceptable salts are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: ApplicationFiled: June 23, 2006Publication date: September 2, 2010Applicant: MERCK & CO., INC.Inventors: Scott E. Wolkenberg, Zhijian Zhao, Craig W. Lindsley
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Publication number: 20100222357Abstract: The present invention relates to indol-3-yl-carbonyl-piperidin and piperazin derivatives which act as V1a receptor antagonists and which are represented by Formula I: wherein the residues R1 to R3 are as defined herein. The invention also relates to pharmaceutical compositions containing such compounds, and methods for preparation of the compounds and compositions. The invention further relates to methods for treating dysmenorrhea, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, obsessive compulsive disorder, anxiety and depressive disorders.Type: ApplicationFiled: May 13, 2010Publication date: September 2, 2010Inventors: Caterina Bissantz, Christophe Grundschober, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
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Patent number: 7786129Abstract: The present invention is concerned with new 3,3-disubstituted indol-2-one derivatives of the general Formula (I), wherein R1 stands for hydrogen, halogen, alkyl having 1-7 carbon atom(s) or sulfonamido; R2 represents hydrogen or halogen; R3 denotes hydrogen, alkyl having 1-7 carbon atom(s) optionally carrying an aryl substituent or aryl optionally carrying one or two halogen substituent(s); R4 stands for alkyl having 1-7 carbon atom(s); R5 represents a group of the general Formula (II a) or (II b), wherein Q and W each represents nitrogen or CH; R6, R7 and R8 each stands for hydrogen, halogen, trifluoromethyl, alkyl or alkoxy having 1-7 carbon atom(s), or R6 and R7 together represent ethylenedioxy; m is 0, 1, or 2; a is a single, double or triple bond; n is 0, 1 or 2; and pharmaceutically acceptable acid addition salts thereof which are useful in the treatment or prophylaxis of diseases of the central nervous system, the gastrointestinal system and the cardiovascular system.Type: GrantFiled: May 11, 2005Date of Patent: August 31, 2010Assignee: Egis Gyogyszergyar NyrtInventors: Balázs Volk, József Barkóczy, Gyula Simig, Tibor Mezei, Rita Kapillerné Dezsöfi, Endréné Flórian, István Gacsályi, Katalin Pallagi, Gábor Gigler, György Lévay, Krisztina Móricz, Csilla Leveleki, Nóra Sziray, Gábor Szénási, András Egyed, László Gábor Hársing
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Publication number: 20100210662Abstract: The present invention relates to 3-disubstituted indol-2-one derivatives, to their preparation and to their therapeutic application.Type: ApplicationFiled: February 9, 2010Publication date: August 19, 2010Applicant: SANOFI-AVENTISInventors: Marco BARONI, Letizia PULEO
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Publication number: 20100210635Abstract: Compounds, pharmaceutical compositions, kits and methods are provided for use with Renin that comprise a compound selected from the group consisting of: wherein the variables are as defined herein.Type: ApplicationFiled: March 23, 2007Publication date: August 19, 2010Applicant: Takeda Pharmaceutical Company LimitedInventors: Benjamin Jones, Andre A. Kiryanov, Stephen W. Kaldor
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Publication number: 20100197673Abstract: The present invention relates to indole or indazole compounds, pharmaceutically acceptable salts or isomers thereof which are useful for the prevention or treatment of cellular necrosis and necrosis-associated diseases. The present invention also relates to a method and a composition for the prevention or treatment of cellular necrosis and necrosis-associated diseases, comprising said indole or indazole compounds as an active ingredient.Type: ApplicationFiled: August 18, 2008Publication date: August 5, 2010Applicant: LG Life Sciences LtdInventors: Soon Ha Kim, Hyoung Jin Kim, Sun Young Koo, Chul Woong Chung, Sung Bae Lee, Heui Sul Park, Seung Hyun Yoon, Hyo Shin Kwak, Dong Ook Seo, Eok Park
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Publication number: 20100197687Abstract: There is provided compounds of formula I, wherein T, Y, X1, R1, R2, R3, R4 and R5 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of the activity of a member of the MAPEG family is desired and/or required, and particularly in the treatment of inflammation.Type: ApplicationFiled: December 22, 2005Publication date: August 5, 2010Inventors: Benjamin Pelcman, Kristofer Olofsson, Martins Katkevics, Vita Ozola, Edgars Suna, Ivars Kalvins, Peteris Trapencieris, Dace Katkevica, Wesley Schaal
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Publication number: 20100190768Abstract: The present invention relates to a compound represented by the formula (1) which is useful as a glucocorticoid receptor function regulating agent, an anti-inflammatory agent or an antidiabetic agent, or a pharmaceutically acceptable salt thereof: wherein R1 is aralkyl, etc.; R2 is H, etc.; —W4?W5—W6?W7— is a group of the formula: —CR4?CR5—CR6?CR7— (in which R4, R5, R6 and R7 are independently a group of the formula: -E-A (E is a single bond, etc., A is H or nitro, etc.)), etc.; R8 is a group of the formula: —OR11 (R11 is H, etc.), etc.; R9 is trifluoromethyl, etc.; R10 is a group of the formula: —[C(R13)(R14)]n—R15 (R13 and R14 are independently H, etc., n is an integer of 0 to 10, R15 is a group of the formula: N(R18)R19 (R18 and R19 form a nitrogen-containing heteromonocycle together with a nitrogen atom to which they are bonded), etc.).Type: ApplicationFiled: September 29, 2006Publication date: July 29, 2010Applicant: Dainippon Sumitomo Pharma Co., Ltd.Inventors: Toshihiko Sone, Rieko Sawaki, Tomoko Nakajima
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Publication number: 20100184750Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.Type: ApplicationFiled: January 18, 2010Publication date: July 22, 2010Applicant: ABBOTT LABORATORIESInventors: Laura A. Hexamer, Hong Ding, Steven W. Elmore, Aaron R. Kunzer, Xiaohong Song, Andrew J. Souers, Gerard M. Sullivan, Zhi-Fu Tao, Michael D. Wendt
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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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Patent number: 7754724Abstract: Novel N-alkyl substituted piperazines have been discovered, which are useful as insecticides or fungicides. Such compounds are of Formula (I) wherein X, Y, R1 and R2 are as defined herein.Type: GrantFiled: June 30, 2006Date of Patent: July 13, 2010Assignee: Dow AgroSciences LLCInventors: Beth Anne Lorsbach, James Melvin Ruiz, Thomas Clarence Sparks, Michael Thomas Sullenberger, Irene Mae Morrison, Jeffery Dale Webster
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Patent number: 7754725Abstract: Compounds having the formula (I): and in particular, those of subgenus VIIa are disclosed as inhibits or modulators of the activity of the heat shock protein Hsp90. As such they are useful for treating cancer, particularly hematopoietic tumors of lymphoid or myeloid lineage, prostate cancer, lung cancer, gastrointestinal stromal tumor, breast cancer and melanoma.Type: GrantFiled: March 1, 2007Date of Patent: July 13, 2010Assignee: Astex Therapeutics Ltd.Inventors: Gianni Chessari, Maria Grazia Carr, Miles Stuart Congreve, Robert Downham, Martyn Frederickson, Christopher William Murray, Eva Figueroa Navarro, Michael Alistair O'Brien, Theresa Rachel Phillips, Andrew James Woodhead
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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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Publication number: 20100160322Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.Type: ApplicationFiled: December 4, 2009Publication date: June 24, 2010Applicant: ABBOTT LABORATORIESInventors: Milan Bruncko, Yujia Dai, Hong Ding, George A. Doherty, Steven W. Elmore, Lisa Hasvold, Laura Hexamer, Aaron Kunzer, Robert A. Mantei, William J. McClellan, Chang H. Park, Cheol-Min Park, Andrew M. Petros, Xiaohong Song, Andrew J. Souers, Gerard M. Sullivan, Zhi-Fu Tao, Gary T. Wang, Le Wang, Xilu Wang, Michael D. Wendt
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Patent number: 7741326Abstract: Compounds of formula I or formula II: or pharmaceutically acceptable salts thereof, wherein m, n, p, Ar R1, R2, R4, and R5 are as defined herein. The invention also provides methods for preparing, compositions comprising, and methods for using compounds.Type: GrantFiled: November 8, 2007Date of Patent: June 22, 2010Assignee: Roche Palo Alto LLCInventors: Joe Timothy Bamberg, Counde O'Yang, Meng Sui, Shu-Hai Zhao
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Publication number: 20100152184Abstract: The invention provides a compound for use in medicine, the compound being a compound of the formula (VI0) or a salt, solvate, tautomer or N-oxide thereof: wherein the bicyclic group: is selected from the structures C1, C5 and C6: wherein n is 0, 1, 2 or 3; R1 is hydrogen, hydroxy, or O—Rz; R2a is hydroxy, methoxy or O—Rz; provided that at least one of R1 and R2a is O—Rz; Rz is Lp-Rp1; SO3H; a glucuronide residue; a mono-, di- or tripeptide residue; or Lp is a bond, C?O, (C?O)O, (C?O)NRp1 or S(O)xNRp1; x is 1 or 2; Rp1 is hydrogen or a an optionally substituted C1-25 hydrocarbyl group containing 0, 1 or 2 carbocyclic rings and 0, 1, 2, 3, 4, 5 or 6 carbon-carbon multiple bonds, provided that Rp1 is not hydrogen when Lp is a bond, C?O or (C?O)O; and provided also that O—Rz does not contain an O—O moiety; and excluding compounds wherein R1 is hydroxy and R2a is methoxy; Rp2 and Rp3 are the same or different and each is a group Rp1; and R3, R4a, R8 and R10 are defined in the claims.Type: ApplicationFiled: October 12, 2007Publication date: June 17, 2010Applicant: ASTEX THERAPEUTICS LIMITEDInventors: Miles Stuart Congreve, Lynsey Helen Fazal, Martyn Frederickson, Christopher William Murray, Michael Alistair O'Brien, Andrew James Woodhead, John Francis Lyons, Neil Thomas Thompson
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Patent number: 7737150Abstract: The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts thereof, wherein: R3 is tert-butylmethyl, sec-butyl or tert-butyl; X is CH or N; and R4 is optionally substituted C1-8 alkyl or optionally substituted C3-8 cycloalkyl. The invention further relates to pharmaceutical compositions comprising compounds of formula (I), and the use of such compounds in the treatment of a disease selected from osteoporosis, Paget's disease, Chagas's disease, malaria, gingival diseases, hypercalaemia, metabolic bone disease, diseases involving matrix or cartilage degradation, and bone cancer disorders such as bone metastases and associated pain.Type: GrantFiled: January 8, 2009Date of Patent: June 15, 2010Assignee: Amura Therapeutics LimitedInventors: Martin Quibell, John Paul Watts
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Publication number: 20100145036Abstract: The present disclosure provides drug-ligand conjugates and drug-cleavable substrate conjugates that are potent cytotoxins. The disclosure is also directed to compositions containing the drug-ligand conjugates, and to methods of treatment using them.Type: ApplicationFiled: December 28, 2007Publication date: June 10, 2010Applicant: Medarex, Inc.Inventors: Bilal Sufi, Vincent Guerlavais, Liang Chen, Sanjeev Gangwar, Qian Zhang, David B. Passmore
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Publication number: 20100130468Abstract: The invention is directed to novel indole carboxamide derivatives. Specifically, the invention is directed to compounds according to formula (I): wherein R1, R2, R3, R4, and m are as defined herein. The compounds of the invention are inhibitors of IKK2 and can be useful in the treatment of disorders associated with inappropriate IKK2 (also known as IKK?) activity, such as rheumatoid arthritis, asthma, rhinitis, and COPD (chronic obstructive pulmonary disease). Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting IKK2 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.Type: ApplicationFiled: March 20, 2008Publication date: May 27, 2010Inventors: Jeffrey Charles Boehm, Jakob Busch-Petersen, Wei Fu, Qi Jin, Jeffrey K. Kerns, Huijie Li, Guoliang Lin, Xichen Lin, Christopher E. Neipp
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Publication number: 20100125075Abstract: Compounds of formula (II) are antibacterial agents wherein Q represents a radical of the formula: —N(OH)CH(?O) or the formula: —C(?O)NH(OH); R1 represents hydrogen, C1-C6 alkyl or C1-C6 alkyl substituted by one or more halogen atoms, or, except when Q is a radical of the formula: —N(OH)CH(?O), a hydroxy, C1-C6 alkoxy, C1-C6 alkenyloxy, amino, C1-C6 alkylamino, or di-(C1-C6 alkylamino group; R2 represents a substituted or unsubstituted C1-C6 alkyl, cycloalkyl(C1-C6 alkyl)- or aryl(C1-C6 alkyl)-group; and A represents a group of formula (IIA), or (IIB) wherein R4 represents the side chain of a natural or non-natural alpha amino acid, and R5 and R6 when taken together with the nitrogen atom to which they are attached form a saturated heterocyclic first ring of 5 to 7 atoms as specified in the description.Type: ApplicationFiled: December 14, 2006Publication date: May 20, 2010Applicant: British Biotech Pharmaceuticals Ltd.Inventors: Lisa Marie Pratt, Kenneth Noel Keavey, Gilles Denis Pain, Laurent Mounier
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Publication number: 20100120749Abstract: The present invention is related to tetrahydroindole derivatives of Formula (I), pharmaceutical composition thereof, methods of preparation thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase).Type: ApplicationFiled: March 28, 2008Publication date: May 13, 2010Applicant: GENKYO TEX SAInventors: Patrick Page, Mike Orchard, Laeticia Fioraso-Cartier, Bianca Mottironi
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Publication number: 20100120740Abstract: The invention relates to prodrugs of fused heterocyclic inhibitors of D-amino oxidase (DAAO) and methods of treating diseases and conditions, wherein modulation of D-amino acid oxidase activity, D-serine levels, D-serine oxidative products and NMDA receptor activity in the nervous system of a mammalian subject is effective.Type: ApplicationFiled: August 6, 2009Publication date: May 13, 2010Applicant: SEPRACOR INC.Inventors: Michele L. R. Heffernan, Richard Dennis, James M. Dorsey, Robert J. Foglesong, Michael L. Jones, Cyprian O. Ogbu, Mustapha Soukri, Kerry L. Spear, H. Scott Wilkinson, Michael Anthony Orsini
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Publication number: 20100120769Abstract: The present invention relates to compounds of formula I wherein s, R1a and R1 to R3 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.Type: ApplicationFiled: January 20, 2010Publication date: May 13, 2010Inventors: Matthias Nettekoven, Jean-Marc ` Plancher, Olivier Roche, Tadakatsu Takahashi, Sven Taylor
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Patent number: 7714146Abstract: The invention is related to novel azulene-oxindole compounds having formula (I) shown below, wherein one of R1, R2 and R3 represents a moiety of formula (II), each of A1 and A2 independently is nitrogen, oxygen or sulfur, each of the others of R1, R2, R3, R1, R5, R6, R7, R8, R9, R10, R11, R12, R13, and R14 is as recited in the specification. The novel compound potentially inhibits multiple kinases and thus can be used to treat some disease like cancer or inflammatory.Type: GrantFiled: October 31, 2007Date of Patent: May 11, 2010Assignee: Industrial Technology Research InstituteInventors: On Lee, Chrong-Shiong Hwang, Chih-Hung Chen, Yuan-Jang Tsai, Chih-Peng Liu, Ching-Huai Ko, Hsin-Hsin Shen, Ling-Mei Wang, Kuei-Tai Lai, Ying-Chu Shih, Ting-Shou Chen, Yen-Chun Chen, Lain-Tze Lee
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Publication number: 20100113424Abstract: The present invention relates to a compound of formula I wherein Ar, R1, R2, R3, n, and o are as defined herein or to a pharmaceutically active salt, a racemic mixture, an enantiomer, an optical isomer or a tautomeric form thereof. The present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).Type: ApplicationFiled: October 23, 2009Publication date: May 6, 2010Inventors: Caterina Bissantz, Philippe Jablonski, Henner Knust, Matthias Nettekoven, Hasane Ratni, Claus Riemer
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Patent number: 7709467Abstract: Compounds which inhibit the activity of anti-apoptotic family protein members, compositions containing the compounds and methods of treating diseases during which occur expression one or more than one of an anti-apoptotic family protein member are disclosed.Type: GrantFiled: May 15, 2008Date of Patent: May 4, 2010Assignee: Abbott LaboratoriesInventors: Milan Bruncko, Hong Ding, Steven W. Elmore, Aaron R. Kunzer, Christopher L. Lynch, William J. McClellan, Cheol Min Park, Xiahong Song, Xilu Wang
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Patent number: 7705023Abstract: There is provided a compound of formula: (I), wherein X, R1, R2, R3, R4, R5 and R6 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of the activity of microsomal prostaglandin E synthase-1 is desired and/or required, and particularly in the treatment of inflammation.Type: GrantFiled: June 17, 2005Date of Patent: April 27, 2010Assignee: Biolipox ABInventors: Kristofer Olofsson, Benjamin Pelcman, Ivars Kalvins, Edgars Suna, Vita Ozola, Martins Katkevics
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Patent number: 7700586Abstract: The present invention relates to a sulfonamide derivative which is useful as an active ingredient of pharmaceutical preparations. The sulfonamide derivatives of the present invention have CCR3 (CC type chemokine receptor) antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with CCR3 activity, in particular for the treatment of asthma, atopic dermatitis, allergic rhinitis and other inflammatory/immunological disorders.Type: GrantFiled: September 4, 2002Date of Patent: April 20, 2010Assignee: Axikin Pharmaceuticals, Inc.Inventors: Yingfu Li, Akihiko Watanabe, Timothy B. Lowinger, Kevin Bacon, Norihiro Kawamura, Takuya Shintani, Tetsuo Kikuchi, Toshiya Moriwaki, Klaus Urbahns, Keiko Fukushima, Noriko Nunami, Takashi Yoshino, Toshiki Murata, Megumi Yamauchi, Hiroko Yoshino