1,2-diazole Ring (including Hydrogenated) Patents (Class 544/140)
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Publication number: 20120213806Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, Z, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.Type: ApplicationFiled: February 16, 2012Publication date: August 23, 2012Applicant: THERAVANCE, INC.Inventors: Melissa Fleury, Roland Gendron, Adam D. Hughes
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Publication number: 20120202816Abstract: The present invention discloses a novel thyroid like compounds of formula (I), wherein R1 R2, R3, R4 and Z are as defined in the specification, method for its preparation, composition containing such compounds and use of such compounds and composition as medicament. Further, compounds of formula (I) has significantly low binding affinity to thyroid receptors and thus considerably devoid of thyrotoxic effects. The invention also relates to the use of the compound of formula (I) for the preparation of a medicament for treating various disease conditions such as obesity, dyslipidemia, metabolic syndrome and co-morbidities associated with metabolic syndrome.Type: ApplicationFiled: January 10, 2012Publication date: August 9, 2012Applicant: Torrent Pharmaceuticals, Ltd.Inventors: Laxmikant Chhipa, Shitalkumar Pukharaj Zambad, Ramesh Gupta, Davinder Tuli, Ashok Kasundra, Siralee Munshi, M. Amir Siddiqui, Subrat Kumar Bhattamisra, C. Dutt, Vijay Chauthaiwale
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Publication number: 20120202812Abstract: This invention provides compounds of formula I: wherein R1, R2, CY, Y1, Y2, X1, X2, and X3 are as described in the specification. The compounds are inhibitors of PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.Type: ApplicationFiled: April 18, 2012Publication date: August 9, 2012Applicant: Millennium Pharmaceuticals, Inc.Inventors: David P. Cardin, Paul Greenspan, Stepan Vyskocil, Jeffrey Gaulin, Tianlin Xu, Christelle C. Renou
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Publication number: 20120190845Abstract: 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: November 9, 2011Publication date: July 26, 2012Inventors: Arthur R. Gomtsyan, Erol K. Bayburt, Chih-Hung Lee, John R. Koenig, Robert G. Schmidt, Kirill A. Lukin, Gilles Chamboumier, Margaret Chi-Ping Hsu, Robert M. Leanna, Russell D. Cink
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Publication number: 20120190673Abstract: The invention provides a compound of the formula (I): or a salt, solvate, tautomer or N-oxide thereof, wherein M is selected from a group D1 and a group D2: and R?, E, A and X are as defined in the claims. Also provided are pharmaceutical compositions containing the compounds, processes for making the compounds and the use of the compounds in the prophylaxis or treatment of a disease state mediated by a CDK kinase, GSK-3 kinase or Aurora kinase.Type: ApplicationFiled: December 19, 2011Publication date: July 26, 2012Applicant: ASTEX THERAPEUTICS LIMITEDInventors: Valerio BERDINI, Maria Grazia CARR, Adrian Liam GILL, Steven HOWARD, Eva Figueroa NAVARRO, Gary TREWARTHA, David Charles REES, Mladen VINKOVIC, Paul Graham WYATT
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Patent number: 8217038Abstract: The present invention provides novel pyrazolines that are useful as cannabinoid receptor blockers and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, inflammatory disorders, cardiometabolic disorders, hepatic disorders, and/or cancers.Type: GrantFiled: October 7, 2010Date of Patent: July 10, 2012Assignee: Jenrin Discovery, Inc.Inventors: John F. McElroy, Robert J. Chorvat
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Publication number: 20120157386Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.Type: ApplicationFiled: December 14, 2011Publication date: June 21, 2012Applicant: THERAVANCE, INC.Inventors: Cameron SMITH, Melissa FLEURY, Roland GENDRON, Ryan HUDSON, Adam D. HUGHES
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Publication number: 20120142686Abstract: The present invention relates to viral polymerase inhibitors of formula (I), salts, N-oxides, solvates, hydrates, racemates, enantiomers or isomers thereof, processes for their preparation and their use in the treatment of Flaviviridae viral infections such as Hepatitis C virus (HCV) infections:Type: ApplicationFiled: October 20, 2011Publication date: June 7, 2012Inventors: Rosliana Halim, Michael Harding, Richard Hufton, Craig James Morton, Saba Jahangiri, Brett Raymond Pool, Tyrone Pieter Jeynes, Alistair George Draffan, Barbara Frey, Michael John Lilly
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Publication number: 20120130069Abstract: Disclosed are novel indazole derivatives represented by the following Chemical Formula 1 or pharmaceutically acceptable salts, hydrates or solvates thereof, and pharmaceutical compositions for the prevention or treatment of proliferative diseases, containing the same as an active ingredient. Having potent inhibitory effect against protein kinase, such as b-raf, KDR, Fms, Tie2, SAPK2a and Ret, inducing diseases caused by abnormal cell proliferation, the novel indazole derivatives can be used for the prevention or treatment of diseases caused by abnormal cell proliferation.Type: ApplicationFiled: December 4, 2009Publication date: May 24, 2012Inventors: Tae Bo Sim, Jung Beom Son, Hwan Kim, Dong Sik Park, Hwan Geun Choi, Young Jin Ham, Jung Mi Hah, Kyung Ho Yoo, Chang Hyun Oh, So Ha Lee, Jae Du Ha, Sung Yun Cho, Byoung Mog Kwon, Dong Cho Han
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Publication number: 20120129844Abstract: 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: January 26, 2012Publication date: May 24, 2012Inventors: David Buttar, Kevin Michael Foote, Maria-Elena Theoclitou, Andrew Peter Thomas
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Publication number: 20120115868Abstract: The present invention is concerned with novel triazole compounds of formula (I) wherein A, X, Y, u, v, R1, R2, and R3 are as described herein, as well as pharmaceutically acceptable salts thereof. The compounds of present invention have affinity and selectivity for the GABA A ?5 receptor. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as pharmaceuticals.Type: ApplicationFiled: November 2, 2011Publication date: May 10, 2012Inventors: Stephen Deems Gabriel, Andrew Thomas
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Publication number: 20120108584Abstract: Compounds corresponding to the formula (I) as defined in the disclosure, as well as methods for making such compounds, intermediates employed in such methods, pharmaceutical compositions containing the compounds of the invention, and methods of treatment using them.Type: ApplicationFiled: January 11, 2012Publication date: May 3, 2012Applicant: SANOFI-AVENTISInventors: Laurent DUBOIS, Yannick Evanno, Christian Maloizel, Mireille Sevrin
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Patent number: 8168627Abstract: Compounds having the structure (or their salts): are used to treat or reduce the likelihood of acquiring androgen-dependent diseases, such as prostate cancer, benign prostatic hyperplasia, polycystic ovarian syndrome, acne, hirsutism, seborrhea, androgenic alopecia and male baldness. The compounds can be formulated together with pharmaceutically acceptable diluents or carriers or otherwise made into any pharmaceutical dosage form. Combinations with other active pharmaceutical agents are also disclosed.Type: GrantFiled: March 16, 2010Date of Patent: May 1, 2012Assignee: Endorecherche, Inc.Inventors: Fernand Labrie, Rock Breton, Shankar Mohan Singh, Rene Maltais
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Publication number: 20120101078Abstract: Disclosed are a series of neuropeptide Y Y5 receptor ligands, and as such are useful to treat disorders related to mood, stress, ADHD, cognition, stress and dementia.Type: ApplicationFiled: March 19, 2010Publication date: April 26, 2012Applicant: H. Lundbrck A/SInventors: Bin Chen, James Ford Burns, Dario Doller
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Patent number: 8163743Abstract: The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I) and salts thereof. The compounds of the invention are inhibitors of P13-kinase activity.Type: GrantFiled: June 3, 2009Date of Patent: April 24, 2012Assignee: GlaxoGroupLimitedInventors: Ian Robert Baldwin, Kenneth David Down, Paul Faulder, Simon Gaines, Julie Nicole Hamblin, Katherine Louise Jones, Joelle Le, Christopher James Lunniss, Nigel James Parr, Timothy John Ritchie, Christian Alan Paul Smethurst, Yoshiaki Washio
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Patent number: 8163729Abstract: The present invention provides compounds of formula (I) and compositions thereof, methods of making them, and methods of using them to modulate alpha7 nicotinic acetylcholine receptors and/or to treat any of a variety of disorders, diseases, and conditions. Provided compounds can affect, among other things, neurological, psychiatric and/or inflammatory system.Type: GrantFiled: January 16, 2008Date of Patent: April 24, 2012Assignees: Wyeth, Siena Biotech S.p.A.Inventors: Chiara Ghiron, Arianna Nencini, Iolanda Micco, Riccardo Zanaletti, Laura Maccari, Hendrick Bothmann, Simon N. Haydar, Maurizio Varrone, Carmela Pratelli, Boyd L. Harrison
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Patent number: 8148372Abstract: Compounds in accord with Formula I: wherein R1, R2, R3 and R4 are as defined in the specification, pharmaceutically acceptable salts, methods of making, pharmaceutical compositions containing and methods for using the same.Type: GrantFiled: August 20, 2010Date of Patent: April 3, 2012Assignee: AstraZeneca ABInventors: Joseph Cacciola, James Empfield, James Folmer, Angela M Hunter, Scott Throner
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Publication number: 20120077796Abstract: The present invention relates to phenalkylamine derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such phenalkylamine derivatives, and the use of such phenalkylamine derivatives for therapeutic purposes. The phenalkylamine derivatives are GlyT1 inhibitors.Type: ApplicationFiled: August 10, 2011Publication date: March 29, 2012Applicants: Abbott Laboratories, Abbott GmbH & Co. KGInventors: Frauke POHLKI, Udo Lange, Wilhelm Amberg, Michael Ochse, Berthold Behl, Charles W. Hutchins, Wilfried Hornberger, Mario Mezler, Sean Turner
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Patent number: 8143424Abstract: A novel thyroid like compounds of formula (I), wherein R1, R2, R3, R4 and Z are as defined in the specification, method for its preparation, composition and use thereof. Further, compounds of formula (I) has significantly low binding affinity to thyroid receptors and thus considerably devoid of thyrotoxic effects. The invention also relates to the use of the compound of formula (I) for the preparation of a medicament for treating various disease conditions including obesity, dyslipidemia, metabolic syndrome and co-morbidities associated with metabolic syndrome.Type: GrantFiled: June 2, 2008Date of Patent: March 27, 2012Assignee: Torrent Pharmaceuticals Ltd.Inventors: Laxmikant Chhipa, Shitalkumar Pukharaj Zambad, Ramesh Gupta, Davinder Tuli, Ashok Kasundra, Siralee Munshi, M. Amir Siddiqui, Subrat Kumar Bhattamisra, Chaitanya Dutt, Vijay Chauthaiwale
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Patent number: 8138186Abstract: 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: GrantFiled: March 2, 2007Date of Patent: March 20, 2012Assignee: Laboratorios Del Dr. Esteve, S.A.Inventors: Rosa Cuberes-Altisent, Joerg Holenz
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Publication number: 20120065196Abstract: The present invention provides compounds represented by the formula (Ie): and the formula (If): wherein each symbol is as defined in the specification. According to the present invention, these compounds have a DGAT inhibitory activity and are useful for the prophylaxis, treatment or improvement of diseases or pathologies caused by high expression or high activation of DGAT.Type: ApplicationFiled: July 20, 2007Publication date: March 15, 2012Inventors: Shuji Kitamura, Thomas Daniel Aicher, Steve Gonzales, Yvan Le Huerou, Scott Alan Pratt, Yoshihisa Nakada
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Publication number: 20120065191Abstract: The invention relates to compounds and compositions for inhibiting the enzyme fatty acid amide hydrolase (FAAH), the use of the compounds in therapy and, in particular, for treating or preventing conditions whose development or symptoms are linked to substrates of the FAAH enzyme, and methods of treatment or prevention using the compounds and compositions.Type: ApplicationFiled: December 23, 2009Publication date: March 15, 2012Applicant: BIAL - PORTELA & CĂ‚ÂŞ, S.A.Inventors: Laszlo Erno Kiss, David Alexander Learmonth, Carla PatrĂcia da Costa Pereira Rosa, Rita GusmĂŁo de Noronha, Pedro Nuno Leal Palma, PatrĂcio Manuel Vieira AraĂşjo Soares da Silva, Alexander Beliaev
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Publication number: 20120046280Abstract: Disclosed are biologically active hetero pyrrole analogs such as imidazoles, thiazoles, oxazoles and pyrazoles capable of interacting with the CB1 and/or CB2 cannabinoid receptors. Aspects disclose hetero pyrrole analogs acting as CB1 and/or CB 1 receptor antagonists, having selectivity for the CB 1 or CB2 receptor, acting as neutral antagonists, acting preferentially on CB 1 receptors located in the peripheral nervous system, and/or acting as nitric oxide donors. Pharmaceutical preparations employing the disclosed analogs and methods of administering therapeutically effective amounts of the disclosed analogs to provide a physiological effect are also disclosed.Type: ApplicationFiled: February 19, 2009Publication date: February 23, 2012Inventors: Alexandros Makriyannis, Venkata K. Vemuri, Teresa Olszewska
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Patent number: 8114899Abstract: Compounds corresponding to the formula (I) as defined in the disclosure, as well as methods for making such compounds, intermediates employed in such methods, pharmaceutical compositions containing the compounds of the invention, and methods of treatment using them.Type: GrantFiled: January 27, 2009Date of Patent: February 14, 2012Assignee: Sanofi-AventisInventors: Laurent DuBois, Yannick Evanno, Christian Maloizel, Mireille Sevrin
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Publication number: 20120029192Abstract: This invention relates to pyrazole derivatives of formula (I) or pharmaceutically acceptable salts, solvates or derivatives thereof, and to processes for the preparation thereof, intermediates used in their preparation of, compositions containing them and the uses of such derivatives. The compounds of the present invention bind to the enzyme reverse transcriptase and are modulators, especially inhibitors thereof. As such, the compounds of the present invention are useful in the treatment of a variety of disorders including those in which the inhibition of reverse transcriptase is implicated. Disorders of interest include those caused by Human Immunodificiency Virus (HIV) and genetically related retroviruses, such as Acquired Immune Deficiency Syndrome (AIDS).Type: ApplicationFiled: October 7, 2011Publication date: February 2, 2012Inventors: Lyn Howard Jones, Charles Eric Mowbray, David Anthony Price, Matthew Duncan Selby, Paul Anthony Stupple
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Publication number: 20120028963Abstract: The present invention relates to hydroxamate derivatives, isomers thereof, pharmaceutically acceptable salts thereof, hydrates thereof, or solvates thereof, the use thereof for preparing pharmaceutical compositions, pharmaceutical compositions containing the same, a method of treating disease using the compositions, and a method for preparing the hydroxamate derivatives.Type: ApplicationFiled: March 18, 2010Publication date: February 2, 2012Applicant: CHONG KUN DANG PHARMACEUTICAL CORP.Inventors: Sung Sook Lee, Kyung Joo Lee, Chang Sik Lee, Hyun Mo Yang, Do Hoon Kim, Dae Kyu Choi, Ho Jin Choi, Dal Hyun Kim, In Chang Hwang, Mi Jeong Kim, Byeong Hoon Han
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Publication number: 20120022054Abstract: The present invention concerns novel substituted aryl derivatives, their process of preparation and their use for inhibiting virus replication and for treating viral diseases or disorders such as HIV and/or HCV infection.Type: ApplicationFiled: December 10, 2009Publication date: January 26, 2012Applicant: LABORATOIRE BIODIMInventors: Richard Benarous, Sabine Barbey-Treve, Jean-Marc Paris, Sebastien Berrut, Clarisse Berlioz-Torrent, Stephane Emiliani
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Publication number: 20120015932Abstract: Indazole compounds, processes for their preparation, intermediates usable in these processes, pharmaceutical compositions containing such compounds and their use in therapy.Type: ApplicationFiled: February 24, 2010Publication date: January 19, 2012Inventors: Heather Hobbs, Simon Teanby Hodgson, Yannick Maurice LaCroix, Deborah Needham, Nigel James Parr, Panayiotis Alexandrou Procopiou, Timothy John Ritchie, Michael David Woodrow
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Publication number: 20110312964Abstract: Compounds of the formula I wherein R1a is H; and R1b is C1-C6 alkyl, Carbocyclyl or Het; or R1a and R1b together define a saturated cyclic amine with 3-6 ring atoms; R2a and R2b are H, halo, C1-C4alkyl, C1-C4haloalkyl, C1-C4alkoxy; or R2a and R2b together with the carbon atom to which they are attached form a C3-C6cycloalkyl; R3 is a branched C5-C10alkyl chain, C2-C4haloalkyl or C3-C7cycloalkylmethyl, R4 is Het, Carbocyclyl, optionally substituted as defined in the specification and pharmaceutically acceptable salts, hydrates and N-oxides thereof; are inhibitors of cathepsin S and have utility in the treatment of psoriasis, autoimmune disorders and other disorders such as asthma, arteriosclerosis, COPD and chronic painType: ApplicationFiled: December 18, 2009Publication date: December 22, 2011Applicant: Medivir UK LTDInventors: Susana Ayesa, Anna Karin Belfrage, Björn Classon, Urszula Grabowska, Ellen Hewitt, Vladimir Ivanov, Daniel Jönsson, Pia Kahnberg, Peter Lind, Magnus Nilsson, Lourdes Odén, Mikael Pelcman, Horst Wähling
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Publication number: 20110306599Abstract: Provided is an agent for the treatment or prophylaxis of inflammatory diseases, allergic diseases, autoimmune diseases, transplant rejection or the like. A compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, or a solvate thereof: wherein each symbol is as described in the specification.Type: ApplicationFiled: November 24, 2010Publication date: December 15, 2011Applicant: JAPAN TOBACCO INC.Inventors: Teruhiko INOUE, Tetsudo KAYA, Shinichi KIKUCHI, Koji MATSUMURA, Ritsuki MASUO, Motoya SUZUKI, Michihide MAEKAWA
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Publication number: 20110294808Abstract: Disclosed indazoles compounds that are useful as antagonists of CCR1 activity and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of CCR1 including autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis. Also disclosed are pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: ApplicationFiled: July 18, 2011Publication date: December 1, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Daniel KUZMICH, Can MAO, Alan David SWINAMER, David Smith THOMSON
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Patent number: 8063044Abstract: This invention relates to pyrazole derivatives of formula (I) or pharmaceutically acceptable salts, solvates or derivative thereofs, wherein R1 to R4 are defined in the description, and to processes for the preparation thereof, intermediates used in their preparation of, compositions containing them and the uses of such derivatives. The compounds of the present invention bind to the enzyme reverse transcriptase and are modulators, especially inhibitors thereof. As such the compounds of the present invention are useful in the treatment of a variety of disorders including those in which the inhibition of reverse transcriptase is implicated. Disorders of interest include those caused by Human Immunodeficiency Virus (HIV) and genetically related retroviruses, such as Acquired Immune Deficiency Syndrome (AIDS).Type: GrantFiled: August 25, 2008Date of Patent: November 22, 2011Assignee: Pfizer Inc.Inventors: Lyn Howard Jones, Charles Eric Mowbray, David Anthony Price, Matthew Duncan Selby, Paul Anthony Stupple
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Publication number: 20110281848Abstract: 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: July 29, 2011Publication date: November 17, 2011Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.Inventors: Rosa CUBERES-ALTISENT, Joerg HOLENZ
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Publication number: 20110281868Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein A1, A2, A3 and L are defined in the description. The present invention relates also to methods of making said compounds, and compositions containing said compounds which are useful for inhibiting kinases such as aurora and KDR.Type: ApplicationFiled: May 12, 2011Publication date: November 17, 2011Applicant: ABBOTT LABORATORIESInventors: Michael R. Michaelides, James H. Holms, Douglas H. Steinman
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Publication number: 20110281843Abstract: Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a deregulated protein kinase activity, like cancer.Type: ApplicationFiled: December 15, 2009Publication date: November 17, 2011Applicant: NERVIANO MEDICAL SCIENCES S.r.l.Inventors: Maria Menichincheri, Jay Aaron Bertrand, Chiara Marchionni, Marcella Nesi, Paolo Orsini, Achille Panzeri
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Publication number: 20110275628Abstract: Disclosed is a compound represented by general formula (I) or a pharmaceutically acceptable salt thereof, which is useful as a selective antagonist of a 5-HT2B receptor. The compound and salt are useful for treatment or prevention of various diseases and conditions associated with a 5-HT2B receptor.Type: ApplicationFiled: November 24, 2009Publication date: November 10, 2011Inventors: Tatsuya Yamagishi, Kiyoshi Kawamura, Tadashi Inoue, Yuji Shishido, Hiroaki Ito
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Publication number: 20110269757Abstract: The present invention is related to pyrazolo pyridine derivatives of Formula (I), pharmaceutical composition 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: September 22, 2009Publication date: November 3, 2011Applicant: GENKYOTEX SAInventors: Patrick Page, Mike Orchard, Benoit Laleu, Francesca Gaggini
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Publication number: 20110257178Abstract: The present invention provides novel pyrazolines that are useful as cannabinoid receptor blockers and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, inflammatory disorders, cardiometabolic disorders, hepatic disorders, and/or cancers.Type: ApplicationFiled: October 7, 2010Publication date: October 20, 2011Applicant: JENRIN DISCOVERYInventors: John F. McElroy, Robert J. Chorvat
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Publication number: 20110237783Abstract: Pharmaceutical compositions and compounds are provided. The compounds of the invention demonstrate anti-proliferative activity, and may promote apoptosis in cells lacking normal regulation of cell cycle and death. In one embodiment of the invention, pharmaceutical compositions of the compounds in combination with a physiologically acceptable carrier are provided. The pharmaceutical compositions are useful in the treatment of hyperproliferative disorders, which disorders include tumor growth, lymphoproliferative diseases, angiogenesis. The compounds of the invention are substituted pyrazoles and pyrazolines.Type: ApplicationFiled: December 23, 2010Publication date: September 29, 2011Applicant: Valocor Therapeutics, Inc.Inventors: Zaihui Zhang, Timothy S. Daynard, Mikhail A. Chafeev, Shisen Wang, Gregory B. Chopiuk, Serguei V. Sviridov
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Patent number: 8022059Abstract: A compound of the formula: wherein ring X is benzene or pyridine; R1 is substituted alkyl; R2 is optionally substituted aryl or optionally substituted heterocyclic group; R3 is hydrogen or alkyl; R4 is hydrogen, halogen or alkyl; R5 is hydrogen or alkyl; R6 and R7 are the same or different and each hydrogen or halogen, or a pharmaceutically acceptable salt thereof, which is useful as IKur blocker effective for preventing or treating cardiac arrhythmia such as atrial fibrillation.Type: GrantFiled: September 26, 2008Date of Patent: September 20, 2011Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Tetsuo Yamaguchi, Hiroyuki Kawanishi, Hideki Ushirogochi, Tatsuyuki Takahashi, Tohru Takebe
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Patent number: 7989485Abstract: 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: GrantFiled: March 5, 2007Date of Patent: August 2, 2011Assignee: Laboratorios del Dr. Esteve, S.A.Inventors: Rosa Cuberes-Altisent, Joerg Holenz
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Publication number: 20110183973Abstract: The invention is directed to certain novel compounds directed to compounds of formula (I) and salts thereof. The compounds of the invention are inhibitors of PI3-kinase activity.Type: ApplicationFiled: June 3, 2009Publication date: July 28, 2011Inventors: Ian Robert Baldwin, Kenneth David Down, Paul Faulder, Simon Gaines, Julie Nicole Hamblin, Paul Spencer Jones, Joelle Le, Nigel James Parr, Timothy John Ritchie, John Edward Robinson, Juliet Kay Simpson, Christian Alan Paul Smethurst
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Publication number: 20110178083Abstract: Vicinal substituted cyclopropyl compounds which are inhibitors of phosphodiesterase 10 are described as are processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of mammals, including human(s) for central nervous system (CNS) disorders and other disorders which may affect CNS function, for example neurological, neurodegenerative and psychiatric disorders including, but not limited to, those comprising cognitive deficits or schizophrenic symptoms.Type: ApplicationFiled: July 9, 2009Publication date: July 21, 2011Inventors: Amy Ripka, Gideon Shapiro, Richard Chesworth
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Publication number: 20110178063Abstract: The invention is directed to certain novel compounds of formula (I) and salts thereof. The compounds of the invention are inhibitors of PI3-kinase activity.Type: ApplicationFiled: June 3, 2009Publication date: July 21, 2011Applicant: GLAXO GROUP LIMITEDInventors: Ian Robert Baldwin, Kenneth David Down, Paul Faulder, Simon Gaines, Julie Nicole Hamblin, Joelle Le, Christopher James Lunniss, Nigel James Parr, Timothy John Ritchie, John Edward Robinson, Juliet Kay Simpson, Christian Alan Paul Smethurst
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Publication number: 20110172207Abstract: The present invention relates to novel substituted pyrazolamides, methods for their preparation, their use for the treatment and/or prophylaxis of diseases, as well as their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, especially of retroviral diseases, in humans and/or animals.Type: ApplicationFiled: September 16, 2010Publication date: July 14, 2011Applicant: AiCuris Gmbh & Co. KGInventors: Rudolf SCHOHE-LOOP, Reinhold Welker, Arnold Paessens, Marcus Bauser, Friederike Stoll, Frank Dittmer, Kerstin Henninger, Daniela Paulsen, Dieter Lang
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Patent number: 7977477Abstract: The invention provides compounds of the formula (I): The compounds have activity against cyclin dependent kinases, glycogen synthase kinase and Auroa kinases and are therefore useful to treat cancer and viral diseases.Type: GrantFiled: July 5, 2004Date of Patent: July 12, 2011Assignee: Astex Therapeutics, LimitedInventors: Valerio Berdini, Michael Alistair O'Brien, Maria Grazia Carr, Theresa Rachel Early, Eva Figueroa Navarro, Adrian Liam Gill, Steven Howard, Gary Trewartha, Alison Jo-Anne Woolford, Andrew James Woodhead, Paul Wyatt
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Publication number: 20110166343Abstract: To provide thienopyrazole derivatives inhibiting PDE 7 selectively, and therefore, enhance cellular cAMP level. Consequently, the compound is useful for treating various kinds of disease such as allergic diseases, inflammatory diseases or immunologic diseases. The compound is thienopyrazole compound represented by the following formula (I): [wherein, especially, R1 is a cyclohexyl, a cycloheptyl group or a tetrahydropyranyl group; R2 is methyl; R3 is a hydrogen atom; and R4 is a group: —CONR5R6 (in which any one of R5 and R6 is a hydrogen atom)].Type: ApplicationFiled: March 14, 2011Publication date: July 7, 2011Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Hidekazu Inoue, Hidenobu Murafuji, Yasuhiro Hayashi
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Publication number: 20110152250Abstract: Compounds that are antagonists of the VR1 receptor, having formula (I) or a pharmaceutically acceptable salt, prodrug, or salt of a prodrug thereof, wherein A1, A2, A3, A4, R7, R8, R9, X, Y, Z, L, n, and m, are as defined herein, and are useful in disorders prevented or ameliorated by inhibiting the VR1 receptor.Type: ApplicationFiled: September 3, 2010Publication date: June 23, 2011Applicant: ABBOTT LABORATORIESInventors: Arthur Gomtsyan, Erol K. Bayburt, Robert G. Schmidt, JR., Chih-Hung Lee, Brian S. Brown, Tammie K. Jinkerson, John R. Koenig, Jerome F. Daanen, Steven P. Latshaw
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Publication number: 20110144080Abstract: The invention provides compounds of the formula: (I) having protein kinase B inhibiting activity: wherein A is a saturated hydrocarbon linker group containing from 1 to 7 carbon atoms, the linker group having a maximum chain length of 5 atoms extending between R1 and NR2R3 and a maximum chain length of 4 atoms extending between E and NR2R3, wherein one of the carbon atoms in the linker group may optionally be replaced by an oxygen or nitrogen atom; and wherein the carbon atoms of the linker group A may optionally bear one or more substituents selected from oxo, fluorine and hydroxy, provided that the hydroxy group when present is not located at a carbon atom a with respect to the NR2R3 group and provided that the oxo group when present is located at a carbon atom a with respect to the NR2R3 group; E is a monocyclic or bicyclic carbocyclic or heterocyclic group; R1 is an aryl or heteroaryl group; and R2, R3, R4 and R5 are as defined in the claims.Type: ApplicationFiled: December 23, 2004Publication date: June 16, 2011Applicants: ASTEX THERAPEUTICS LIMITED, THE INSTITUTE OF CANCER RESEARCH ROYAL CANCER HOSPITALInventors: Valerio Berdini, Gordon Saxty, Marinus Leendert Verdonk, Steven John Woodhead, Paul Graham Wyatt, Robert George Boyle, Hanna Fiona Sore, David Winter Walker, Ian Collins, Robert Downham, Robin Arthur Ellis Carr
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Publication number: 20110135650Abstract: The present invention provides a compound of Formula (I) as described herein, or a pharmaceutically acceptable salt or a solvate thereof. The present invention also provides pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing a thromboses, embolisms, hypercoagulability or fibrotic changes.Type: ApplicationFiled: June 1, 2010Publication date: June 9, 2011Inventors: Samuel CHACKALAMANNIL, Tin-Yau CHAN, Mariappan V. CHELLIAH, Martin C. CLASBY, Michael DWYER, William J. GREENLEE, Tomokazu HIRABAYASHI, Santhosh NEELAMKAVIL, Hidemitsu NISHIDA, Fumihiko SAITOH, Unmesh SHAH, Yan XIA