Three Or More Hetero Atoms In The Polycyclo Ring System Patents (Class 540/578)
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Publication number: 20110257156Abstract: In its many embodiments, the present invention provides novel heterocyclic compounds as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.Type: ApplicationFiled: November 5, 2009Publication date: October 20, 2011Inventors: Zhaoning Zhu, William J. Greenlee, David James Cole, Dmitri A. Pissarnitski, Gioconda V. Gallo, Hongmei Li, Hubert B. Josien, Jun Qin, Chad E. Knutson, Mihirbaran Mandal, Monica L. Vicarel, Murali Rajagopalan, Pawan Kumar Dhondi, Ruo Xu, Zhong-Yue Sun, Thomas A. Bara, Xianhai Huang, Xiaohong Zhu, Zhiqiang Zhao, John W. Clader, Anandan Palani, Theodros Asberom, Troy McCracken, Chad E. Bennett
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Patent number: 8039460Abstract: Compounds of Formula (I): and Formula (II): (where variables R2, R4, A, B, D, W, X, Y and Z are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.Type: GrantFiled: October 12, 2005Date of Patent: October 18, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Christopher S. Burgey, Daniel V. Paone, Anthony W. Shaw, Diem N. Nguyen, Zhengwu J. Deng, Theresa M. Williams, Joseph P. Vacca, Craig M. Potteiger, Harold G. Selnick
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Publication number: 20110245234Abstract: The present invention is directed to a compound of formula (I): or a crystalline form thereof, or a solvate thereof; to a solid pharmaceutical composition comprising a pharmaceutically effective amount of the compound of formula (I), or a crystalline form thereof, or a solvate thereof, and at least one pharmaceutically acceptable carrier or diluent, and to the use of a compound of formula (I), or a crystalline form thereof, or a solvate thereof, for treating a patient suffering from, or subject to, a disease, disorder, or condition mediated by Aurora kinase, and methods related thereto.Type: ApplicationFiled: February 15, 2011Publication date: October 6, 2011Applicant: Millennium Pharmaceuticals, Inc.Inventors: Ian Armitage, Martin I. Cooper, Mark D. Eddleston, Neil C. Faiber, Quentin J. McCubbin, Stephen W. Watt
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Publication number: 20110230468Abstract: Fused heterocylic compounds of the following Formula wherein R1, R2, R5, Z, J1 and J2 are described herein, and analogs thereof are provided which are useful in treating leukocyte activation-associated disorders.Type: ApplicationFiled: June 1, 2011Publication date: September 22, 2011Inventors: Joseph Barbosa, William J. Pitts, Junqing Guo
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Publication number: 20110230460Abstract: The invention relates to new thienotriazolodiazepine derivatives of the formula (1) wherein R1 is CH3, R2 is CH3 or —(CH2)n—R4 or —(CH2)n—O—R4 or —(CH2)n—S—R4 wherein n is 1, 2, 3 or 4 and R4 is CH3, CH2CH3 or CH2CH2OCH3, and R3 is hydrogen or —OCH2O— or —OCH2CH2O— connected to the ortho/meta position or meta/para position of the phenyl ring; or wherein R1 and R2 are hydrogen and R3 is —OCH2O— Or —OCH2CH2O— connected to the ortho/meta position or meta/para position of the phenyl ring; and pharmaceutically acceptable acid addition salts thereof. These compounds and pharmaceutical compositions containing them are useful in the treatment and prevention of atherosclerotic artery diseases, such as myocardial infarction and stroke, and of Alzheimer's disease.Type: ApplicationFiled: October 29, 2009Publication date: September 22, 2011Applicant: CircoMed LLCInventors: Herman Kempen, Daniel Bellus, Barbara Staehelin
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Patent number: 8022061Abstract: Compounds having formula I: where A1, A2, L, V, W, R1, R2, R3, R4 and R5 are as described herein, compositions thereof, and their use for the treatment or prevention of type 2 diabetes and type 2 diabetes-related conditions are provided herein.Type: GrantFiled: October 9, 2007Date of Patent: September 20, 2011Assignee: Amgen Inc.Inventors: Yasuyuki Ogawa, Ryo Okuyama, Satoshi Shibuya, Narihiro Toda, Zhaodan Cao, Zice Fu, Xiaolin Hao, Yong-Jae Kim, Leping Li, Sarah E. Lively, Mike Lizarzaburu, Hui Tian, Ming Yu
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Patent number: 8012957Abstract: This invention is directed to a tetrahydro-1H-1,2,6-triaza-azulene cannabinoid modulator compound of formula (I): and a method for use in treating, ameliorating or preventing a cannabinoid receptor mediated syndrome, disorder or disease.Type: GrantFiled: March 27, 2007Date of Patent: September 6, 2011Assignee: Janssen Pharmaceutica NVInventors: Mingde Xia, Fina Liotta, Michael P. Wachter
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Publication number: 20110212942Abstract: The present invention provides compounds having a structure according to Formula (I): or a salt or solvate thereof, wherein ring A, X, R1, R2, R3, R4, R5 and R6 are defined herein. The invention further provides pharmaceutical compositions including the compounds of the invention and methods of making and using the compounds and compositions of the invention, e.g., in the treatment and prevention of various disorders, such as Parkinson's disease.Type: ApplicationFiled: December 21, 2010Publication date: September 1, 2011Inventors: Robert A. Galemmo, Dean R. Artis, Xiaocong Michael Ye, Danielle Aubele, Anh Truong, Simeon Bowers, Roy K. Hom, Yong-Liang Zhu, R. Jeffrey Neitz, Jennifer Sealy, Marc Adler, Paul Beroza, John P. Anderson
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Publication number: 20110207716Abstract: The present invention provides compounds having a structure according to Formula (I): or a salt or solvate thereof, wherein ring A, E1, E2, R1, R2, R3 and R4 are defined herein. The invention further provides pharmaceutical compositions including the compounds of the invention and methods of making and using the compounds and compositions of the invention, e.g., in the treatment and prevention of various disorders, such as Parkinson's disease.Type: ApplicationFiled: December 21, 2010Publication date: August 25, 2011Inventors: Robert A. Galemmo, Dean R. Artis, Xiaocong Michael Ye, Danielle Aubele, Anh Truong, Simeon Bowers, Roy K. Hom, Yong-Liang Zhu, R. Jeffrey Neitz, Jennifer Sealy, Marc Adler, Paul Beroza, John P. Anderson
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Publication number: 20110207717Abstract: Certain 2-aminopyrimidine compounds are serotonin receptor modulators useful in the treatment of diseases mediated by serotonin receptors.Type: ApplicationFiled: October 29, 2009Publication date: August 25, 2011Inventors: Nicholas I. Carruthers, Gregor J. MacDonald, Brock T. Shireman, Vi T. Tran
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Publication number: 20110201804Abstract: Disclosed herein is a process for the manufacture of mirtazapine and intermediates useful in preparing mirtazapine which includes the reduction of 1-(3-carboxypyridyl-2)-4-methyl-2-phenylpiperazine with an organoaluminum hydride.Type: ApplicationFiled: October 20, 2009Publication date: August 18, 2011Applicant: WATSON PHARMA PRIVATE LIMITEDInventors: Manjunath Narayan Bhanu, Samir Naik, Prashant Joshi, Vijay Sharma
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Publication number: 20110195950Abstract: The invention relates to compound of the formula I in which R1 represents an optionally substituted aryl group or an optionally substituted heteroaryl group; R2 represents hydrogen or a substituent different from hydrogen; R3 represents an optionally substituted aryl group, cycloalkyl group, heteroaryl group, heterocyclyl group; X1 represents O, S, NR4, CR42; X2 represents O, S, NR4, CR42; X3 represents O, S, NR4, CR42; X4 represents O, S, NR4, CR42; R4 represents hydrogen or a substituent different from hydrogen; R5 represents hydrogen or alkyl; Y represents O or S; m represents 0, 1, 2 or 3; n represents 0, 1, 2 or 3 in free base form or in acid addition salt form; to its preparation, to its use as medicament and to medicaments comprising it.Type: ApplicationFiled: August 12, 2008Publication date: August 11, 2011Inventors: Samuel Hintermann, Konstanze Hurth, Marina Tintelnot-Blomley
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Patent number: 7994314Abstract: The invention relates to the preparation of mirtazapine precursors and mirtazapine preferably having a substantial enantiomeric excess.Type: GrantFiled: April 7, 2008Date of Patent: August 9, 2011Assignee: N.V. OrganonInventors: Gerardus Johannes Kemperman, Johannes Paulus Gerardus Seerden
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Patent number: 7989444Abstract: Compounds of formula (I) wherein A is a 5 or 6 membered heteroaromatic ring or a 5 or 6 membered heterocyclic ring, and which are useful for treating mental disorders such as schizophrenia are set out herein.Type: GrantFiled: May 31, 2005Date of Patent: August 2, 2011Assignee: Glaxo Group LimitedInventors: Giorgio Bonanomi, Federica Damiani, Gabriella Gentile, Dieter Wolfgang Hamprecht, Fabrizio Micheli, Luca Tarsi, Giovanna Tedesco, Silvia Terreni
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Patent number: 7964590Abstract: The present invention relates to steroidal alkaloids useful in the treatment of hedgehog pathway related disorders, particularly cancer.Type: GrantFiled: March 7, 2008Date of Patent: June 21, 2011Assignee: Infinity Discovery, Inc.Inventors: Alfredo C. Castro, Michael J. Grogan, Andre Lescarbeau, Martin Tremblay
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Publication number: 20110126300Abstract: Provided is a method for high through-put screening for physiologic alterations in an altered teleost displaying a phenotype that is characteristic of the alteration and different from a wild-type, unaltered, matched teleost, comprising the steps of contacting the teleost displaying a genetically-inherited or chemically-induced phenotype with at least one test compound for a sufficient time and under suitable conditions to induce a response in the teleost indicative of pharmacological activity of the compound, and detecting and comparing the response with that of a matched, untreated, control, wherein a change in the teleost signal that is different from that of the control, indicates an altered phenotype and pharmacological activity of the at least one test compound. Further provided are the compounds identified by this method, the zebrafish having an altered phenotype resulting from treatment in accordance with these methods, and kits for facilitating the high through-put screening methods.Type: ApplicationFiled: December 19, 2006Publication date: May 26, 2011Inventor: Michael Pack
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Publication number: 20110118236Abstract: An object of the present invention is to provide a novel AMPA receptor potentiator. A compound represented by the following formula (I) or a salt thereof: wherein in formula (I) R1 represents (1) a halogen atom, or (2) cyano group, or the like; Ra and Rb each independently represent a hydrogen atom or C1-4 alkyl; L represents a bond, or a spacer in which the number of atoms in the main chain is 1 to 8; Ring A represents (1) a non-aromatic carbon ring of 4-8 carbon atoms, or (2) a 4- to 8-membered non-aromatic heterocycle either of which is optionally substituted with 1 or more substituents selected from (a) halogen atoms, and (b) cyano group; and Ar represents a substituted phenyl group, or optionally substituted 5- or 6-membered aromatic heterocyclic group.Type: ApplicationFiled: March 25, 2009Publication date: May 19, 2011Inventors: Michiyo Mochizuki, Shotaro Miura
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Patent number: 7928099Abstract: The present invention provides a compound of formula (I): or a pharmaceutically acceptable salt thereof wherein the variables R1, R2, R3a, R3b, R3b, R3d, and R100 are as defined herein. The invention is also directed to pharmaceutical compositions comprising the compounds of formula (I) and methods of treating a 5-HT2c receptor-mediated disorders with a compound of formula (I) or a pharmaceutical composition comprising a compound of formula (I).Type: GrantFiled: March 14, 2008Date of Patent: April 19, 2011Assignee: Pfizer IncInventors: Mark Andrews, Julian Blagg, Paul Brennan, Paul Fish, R. Ian Storer, Gavin Whitlock
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Publication number: 20110082130Abstract: Piperazinyl oxoalkyl tetrahydroisoquinolines and related analogues of the Formula: are provided, in which variables are as described herein. Such compounds may be used to modulate ligand binding to histamine H3 receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of central nervous system (CNS) and other disorders in humans, domesticated companion animals and livestock animals. Compounds provided herein may be administered alone or in combination with one or more other CNS agents to potentiate the effects of the other CNS agent(s). Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting histamine H3 receptors (e.g., receptor localization studies).Type: ApplicationFiled: August 23, 2010Publication date: April 7, 2011Applicant: LIGAND PHARMACEUTICALS, INC.Inventors: Yang Gao, Bingsong Han, Yuelian Xu, Timothy M Caldwell, Linghong Xie
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Patent number: 7915404Abstract: The present invention is directed to novel processes for the preparation of fused pyrazole compounds, useful for the treatment of disorders and conditions mediated by serotonin receptor activity.Type: GrantFiled: May 4, 2007Date of Patent: March 29, 2011Assignee: Janssen Pharmaceutica NVInventors: Xiaohu Deng, Jimmy T. Liang, Neelakandha Mani
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Patent number: 7897595Abstract: The present invention relates to pyridoazepine derivatives that act as 5-HT ligands, e.g., 5-HT2 C. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.Type: GrantFiled: May 23, 2007Date of Patent: March 1, 2011Assignee: Forest Laboratories Holdings LimitedInventors: Gian-Luca Araldi, Alexander Bischoff, Nhut K. Diep
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Patent number: 7893051Abstract: The present invention generally relates to a series of compounds, to pharmaceutical compositions containing the compounds, and to use of the compounds and compositions as therapeutic agents. More specifically, compounds of the present invention are thiophenyl and pyrrolyl azepine compounds. These compounds are serotonin receptor (5-HT2c) ligands and are useful for treating diseases, disorders, and conditions wherein modulation of the activity of serotonin receptors (5-HT2c) is desired (e.g. addiction, anxiety, depression, obesity, and others).Type: GrantFiled: January 17, 2007Date of Patent: February 22, 2011Assignee: Athersys, Inc.Inventors: L. Nathan Tumey, David C. Bom, Youssef L. Bennani, Michael J. Robarge
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Patent number: 7888347Abstract: The present invention relates to novel pyrazole derivatives of formula I having pharmacological activity as H3 antagonists processes for their preparation, to compositions containing them and to their use in the treatment of neurological and psychiatric disorders.Type: GrantFiled: July 4, 2006Date of Patent: February 15, 2011Assignee: Glaxo Group LimitedInventors: Mark James Bamford, David Matthew Wilson
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Publication number: 20110021493Abstract: This invention relates to novel compounds and processes for their preparation, methods of treating diseases, particularly cancer, comprising administering said compounds, and methods of making pharmaceutical compositions for the treatment or prevention of disorders, particularly cancer.Type: ApplicationFiled: September 2, 2008Publication date: January 27, 2011Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Hartmut Schirok, Ying Li-Sommer, Michael Brands, Mario Lobell, Adrian Tersteegen, Herbert Himmel, Karl-Heinz Schlemmer, Dieter Lang, Kirsten Petersen, Matthias Renz, Dominik Mumberg, Jens Hoffman, Gerhard Siemeister, Ulf Bömer
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Publication number: 20110015175Abstract: The present disclosure provides a series of compounds of the formula (I) which reduce ?-amyloid peptide (?-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by ?-amyloid peptide (?-AP) production.Type: ApplicationFiled: January 7, 2010Publication date: January 20, 2011Inventors: Lawrence R. Marcin, Lorin A. Thompson, III, Kenneth M. Boy, Jason M. Guernon, Mendi A. Higgins, Jianliang Shi, Yong-Jin Wu, Yunhui Zhang, John E. Macor
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Publication number: 20110003793Abstract: Novel MCH-1 receptor antagonists are disclosed. These compounds are used in the treatment of various disorders, including obesity, anxiety, depression, non-alcoholic fatty liver disease, and psychiatric disorders. Methods of making these compounds are also described in the present invention.Type: ApplicationFiled: July 1, 2010Publication date: January 6, 2011Applicant: ALBANY MOLECULAR RESEARCH, INC.Inventors: Peter R. Guzzo, Matthew David Surman, James Francis Grabowski, JR., Emily Elizabeth Freeman
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Publication number: 20110004951Abstract: This invention relates to methods and compositions for identifying compounds that inhibit HIV-1 subunit-specific reverse transcriptase.Type: ApplicationFiled: May 24, 2005Publication date: January 6, 2011Inventors: John C. Kappes, Alok Mulky, Xiaoyun Wu
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Publication number: 20100331310Abstract: Compounds represented by formula (I) and pharmaceutically acceptable salts thereof have excellent sodium channel inhibitory action and are useful as therapeutic agents and analgesics for various kinds of neuralgia, neuropathy, epilepsy, insomnia, premature ejaculation and the like. wherein Q represents ethylene, etc., R1, R2 and R3 represent hydrogen, etc., X1 represents C1-6 alkylene, etc., X2 represents C1-6 alkylene, etc., A1 represents a 5- to 6-membered heterocyclic group, etc., and A2 represents C6-14 aryl, etc.Type: ApplicationFiled: February 9, 2009Publication date: December 30, 2010Inventors: Fumihiro Ozaki, Motohiro Soejima, Tasuku Ishida, Yoshihiko Norimine, Nobuyuki Kurusu, Eriko Doi, Toshihiko Kaneko, Daiju Hasegawa, Kiyoaki Kobayashi, Noboru Yamamoto
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Publication number: 20100324023Abstract: Compounds of Formula I: I (where variables R1A, R1B, R2, R3, R4, A, and Z are as defined herein) useful as antagonists of CGRP receptors, and useful in the treatment or prevention of diseases in which CGRP receptors are involved, such as headache, and in particular migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP receptors are involved.Type: ApplicationFiled: February 6, 2009Publication date: December 23, 2010Applicant: Merck Sharp & Dohme Corp.Inventors: Howard G. Selnick, Ian M. Bell
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Publication number: 20100305102Abstract: The invention relates to new dihydrothienopyrimidinesulphoxides of formula 1, as well as pharmacologically acceptable salts thereof, wherein X is SO or SO2, but preferably SO, and wherein R3 denotes an optionally substituted, mono- or bicyclic, unsaturated, partially saturated or saturated heterocycle or an optionally substituted, mono- or bicyclic heteroaryl and wherein R1 and R2 have the meanings stated in claim 1, as well as pharmaceutical compositions which contain these compounds. These new dihydrothienopyrimidinesulphoxides are suitable for the treatment of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin or eyes, diseases of the peripheral or central nervous system or cancers.Type: ApplicationFiled: October 16, 2008Publication date: December 2, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Pascale Pouzet, Ralf Anderskewitz, Horst Dollinger, Dennis Fiegen, Thomas Fox, Rolf Goeggel, Christoph Hoenke, Domnic Martyres, Peter Nickolaus, Klaus Klinder
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Publication number: 20100292214Abstract: The Invention relates to compounds having an antiparasitic activity, and to their use as a drug, in particular as a drug for the prevention and/or treatment of parasitic diseases caused by apicomplexans. The invention also relates to pharmaceutical compositions containing those compounds.Type: ApplicationFiled: June 2, 2008Publication date: November 18, 2010Applicants: commissariat a l'Energie Atomique, Centre National De La Recherche ScientifiqueInventors: Michael Deligny, Nadia Saidani, Anne-Laure Bonneau, Cyrille Botte, Helene Hardre, Bernard Rousseau, Henri Vial, Corinne Mercier, Roman Lopez, Eric Marechal
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Publication number: 20100292188Abstract: The present invention relates to compounds of formula (I) comprising a cyclobutoxy group, processes for preparing them, pharmaceutical compositions comprising said compounds and their use as pharmaceuticals.Type: ApplicationFiled: January 22, 2009Publication date: November 18, 2010Applicant: UCB PHARMA S.A.Inventors: Frédéric Denonne, Sylvain Celanire, Anne Valade, Sabine Defays, Véronique Durieu
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Publication number: 20100280240Abstract: Antibacterial compounds, compositions containing them, and methods of use for the inhibition of bacterial activity and the treatment, prevention or inhibition of bacterial infection.Type: ApplicationFiled: July 9, 2010Publication date: November 4, 2010Inventors: Brett D. Allison, Laurent Gomez, Cheryl A. Grice, Michael D. Hack, Brain J. Morrow, S. Timothy Motley, Alejandro Santillan, JR., Karen J. Shaw, Kimberly L. Schwarz, Liu Y. Tang, Hariharan Venkatesan, John J.M. Wiener
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Publication number: 20100274004Abstract: Antibacterial compounds, compositions containing them, and methods of use for the inhibition of bacterial activity and the treatment, prevention or inhibition of bacterial infection.Type: ApplicationFiled: July 9, 2010Publication date: October 28, 2010Inventors: Brett D. Allison, Laurent Gomez, Cheryl A. Grice, Michael D. Hack, Brian J. Morrow, S. Timothy Motley, Alejandro Santillan, JR., Karen J. Shaw, Kimberly L. Schwarz, Liu Y. Tang, Hariharan Venkatesan, John J.M. Wiener
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Publication number: 20100274005Abstract: Antibacterial compounds, compositions containing them, and methods of use for the inhibition of bacterial activity and the treatment, prevention or inhibition of bacterial infection.Type: ApplicationFiled: July 9, 2010Publication date: October 28, 2010Inventors: Brett D. Allison, Laurent Gomez, Cheryl A. Grice, Michael D. Hack, Brian J. Morrow, S. Timothy Motley, Alejandro Santillan, JR., Karen J. Shaw, Kimberly L. Schwarz, Liu Y. Tang, Hariharan Venkatesan, John J. M. Wiener
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Publication number: 20100249110Abstract: The present invention relates to substituted pyrazolo-pyrimidine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted pyrazolo-pyrimidine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds or pharmaceutical compositions to subjects in need thereof.Type: ApplicationFiled: March 31, 2010Publication date: September 30, 2010Applicant: ArQule, Inc.Inventors: Manish Tandon, Jianqiang Wang, Nivedita Namdev
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Publication number: 20100249106Abstract: Thiopheneprymidinone compounds useful in therapy, especially for use in the treatment and/or prevention of a steroid hormone dependent disorder, preferably a steroid hormone dependent disease or disorder requiring the inhibition of a 17?-hydroxysteroid dehydrogenase (17?-HSD) such as 17?-HSD type 1, type 2 or type 3 enzyme.Type: ApplicationFiled: June 8, 2010Publication date: September 30, 2010Applicant: SOLVAY PHARMACEUTICALS B.V.Inventors: Kristiina WAEHAELAE, Annamaria Lilienkampf, Sari Alho, Kaisa Huhtinen, Nina Johansson, Pasi Koskimies, Kimmo Vihko
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Publication number: 20100249109Abstract: The present invention relates to substituted tetrahydropyrazolo-pyrido-azepine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted tetrahydropyrazolo-pyrido-azepine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.Type: ApplicationFiled: March 31, 2010Publication date: September 30, 2010Applicant: ArQule, Inc.Inventors: Jean-Marc Lapierre, Rui-Yang Yang, Nivedita Namdev, Jeffrey S. Link
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Publication number: 20100249108Abstract: The present invention relates to substituted dipyrido-pyrimido-diazepine compounds, substituted benzo-pyrido-pyrimido-diazepine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted dipyrido-pyrimido-diazepine compounds, substituted benzo-pyrido-pyrimido-diazepine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.Type: ApplicationFiled: March 31, 2010Publication date: September 30, 2010Applicant: ArQule, Inc.Inventors: Manish Tandon, Yanbin Liu, Nivedita Namdev, Mark A. Ashwell, Rocio Palma
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Publication number: 20100234351Abstract: A compound of the formula: wherein ring A is a 7-membered or 8-membered nitrogen-containing ring optionally further substituted, ring B is an optionally substituted aryl group or an optionally substituted heteroaryl group, X1 is a group represented by —NR3—Y1—, —O—, —S—, —SO—, —SO2— or —CHR3— wherein R3 is a hydrogen atom or an optionally substituted aliphatic hydrocarbon group, or R3 may be bonded to the carbon atom of ring B to form an optionally substituted ring structure, and Y1 is a bond or an optionally substituted alkylene, R1 is a hydrogen atom, or an optionally substituted group bonded via a carbon atom or a sulfur atom, the formula shows a single bond or a double bond, when R2 is —R2, R2 is a hydrogen atom, or an optionally substituted group bonded via a carbon atom, a nitrogen atom, an oxygen atom or a sulfur atom, and when R2 is ?R2, R2 is an oxo group, an optionally substituted alkylidene group, or an optionally substituted imino group.Type: ApplicationFiled: February 22, 2007Publication date: September 16, 2010Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Masaki Seto, Tomohiro Ohashi
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Publication number: 20100222316Abstract: The present invention relates to compounds which are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme for the treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome, and other diseases and conditions that are mediated by excessive glucocorticoid action.Type: ApplicationFiled: March 17, 2010Publication date: September 2, 2010Applicant: ABBOTT LABORATORIESInventors: Marina A. Pliushchev, Dariusz Wodka, Bryan K. Sorensen, James T. Link
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Publication number: 20100216769Abstract: The present invention relates to new substituted glycinamides of general formula (I) wherein D, M, R3, R4 and R5 are defined as in the specification, the tautomers, enantiomers, diastereomers, mixtures and salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.Type: ApplicationFiled: June 28, 2006Publication date: August 26, 2010Inventors: Henning Priepke, Georg Dahmann, Kai Gerlach, Roland Pfau, Wolfgang Wienen, Annette Schuler-Metz, Sandra Handschuh, Herbert Nar
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Publication number: 20100204206Abstract: Di(hetero)arylcyclohexane derivatives, their preparation, their use and pharmaceutical compositions comprising them The present invention relates to di(hetero)arylcyclohexane derivatives of the formula I, in which Ar1, Ar2, R1 and R2 have the meanings indicated in the claims. The compounds of the formula I are valuable pharmaceutical active compounds which inhibit ATP-sensitive potassium channels in the heart muscle and are suitable, for example, for the treatment of disorders of the cardiovascular system such as arrhythmias or a decreased contractility of the heart, such as can occur, for example, in coronary heart disease, cardiac insufficiency or cardiomyopathies. In particular, they are suitable for the prevention of sudden cardiac death. The invention furthermore relates to processes and intermediates for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.Type: ApplicationFiled: December 3, 2009Publication date: August 12, 2010Applicant: SANOFI-AVENTISInventors: Thomas BOHME, Uwe GERLACH, Dirk GRETZKE, Heinz-Werner KLEEMANN, Stefania PFEIFFER-MAREK, Henning VOLLERT, Jean-Michel ALTENBURGER, Sergio MALLART
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Publication number: 20100190687Abstract: The present invention relates to Pyrimidinone Derivatives, compositions comprising a Pyrimidinone Derivative, and methods of using the Pyrimidinone Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of G protein-coupled receptor 119 (“GPR119”) in a patient.Type: ApplicationFiled: April 17, 2008Publication date: July 29, 2010Inventors: Craig D. Boyle, Santhosh Francis Neelamkavil, Samuel Chackalamannil, Bernard R. Neustadt, Jinsong Hao, Unmesh G. Shah, Joel M. Harris, Hong Liu, Andrew W. Stamford
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Publication number: 20100179128Abstract: The present invention relates to compounds of formula (I) which are xanthine derivatives, processes for the manufacture of said derivatives, pharmaceutical formulations containing these active compounds and the use of the compounds in therapy, for example, in the treatment of diseases where under-activation of the HM74A receptor contributes to the disease or where activation of the receptor will be beneficialType: ApplicationFiled: August 8, 2006Publication date: July 15, 2010Inventors: Richard Jonathan Daniel Hatley, Jag Paul Heer, John Liddle, Andrew McMurtrie Mason, Ivan Leo Pinto, Shahzad Sharooq Rahman, Ian Edward David Smith
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Publication number: 20100179319Abstract: The invention provides a process for efficiently producing optically active mirtazapine. Specifically, a process for production of optically active mirtazapine wherein an RS mixture of mirtazapine is optically resolved with optically active tartaric acid in the presence of a solvent. More specifically, a process for production of optically active mirtazapine, characterized by making an RS mixture of mirtazapine contact with optically active tartaric acid in the presence of a solvent, and preferentially crystallizing the optically active mirtazapine salt. The solvent is preferably a mixed solvent consisting of a water-soluble organic solvent and water, and more preferably a mixed solvent consisting of a C1-3 alcohol and water.Type: ApplicationFiled: July 2, 2008Publication date: July 15, 2010Inventors: Weiqi Wang, Tetsuya Ikemoto
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Publication number: 20100168416Abstract: Polycyclic heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.Type: ApplicationFiled: March 9, 2010Publication date: July 1, 2010Applicant: RIGEL PHARMACEUTICALS, INC.Inventors: Dane Goff, Jing Zhang, Rajinder Singh, Sacha Holland, Jiaxin Yu, Thilo J. Heckrodt, Pingyu Ding, Joane Litvak
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Publication number: 20100168082Abstract: The invention relates to novel organic compounds of formula (I) and their use in the treatment of the animal or human body, to pharmaceutical compositions comprising a compound of formula I and to the use of a compound of formula I for the preparation of pharmaceutical compositions for use in the treatment of protein kinase dependent diseases, especially of proliferative diseases, such as in the treatment of tumour diseases and ocular neovascular diseases.Type: ApplicationFiled: December 7, 2009Publication date: July 1, 2010Inventors: Gerald David Artmann, III, Jason Matthew Elliott, Nan Ji, Donglei Liu, Fupeng Ma, Nello Mainolfi, Erik Meredith, Karl Miranda, James J. Powers, Chang Rao
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Patent number: 7732437Abstract: The invention concerns a novel histamine receptor antagonist and the use of an histamine receptor antagonist for the reduction of intracranial pressure (ICP), in particular for the prevention and treatment of elevated intracranial pressure and/or secondary ischaemida, in particular caused by brain injury, more in particular caused by traumatic (TBI) and non-traumatic brain injury. The novel compounds comprise compounds according to the general Formula (I) the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof and the N-oxide form thereof. In particular, the preferred compound is 3-[2-[4-(11,12-dihydro-6H-benzimidazo[2,1-b][3]benzazepin-6-yl)-2-(phenyl-methyl)-1-piperidinyl]ethyl]-2,10-dimethyl pyrimido[1,2-?]benzimidazol-4(10H)-one, the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof and the N-oxide form thereof.Type: GrantFiled: November 22, 2002Date of Patent: June 8, 2010Assignee: Janssen Pharmaceutica, NV.Inventors: Frank Tegtmeier, Frans Eduard Janssens, Joseph Elisabeth Leenaerts, Koenraad Arthur van Rossem, Manuel Jesús Alcázar-Vaca, Pedro Martínez-Jiménez, José Manuel Bartolomé-Nebreda, Antonio Gómez-Sánchez, Francisco Javier Fernández-Gadea, Jozef Leo Henri Van Reempts
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Publication number: 20100137581Abstract: A process for preparation of substantially pure polymorphic Form I of olazapine consists in that olanzapine starting material is subjected to: a) at least one digestion step in an acidic aqueous medium, with an optional addition of active charcoal, and then to neutralizing to pH within the range from about 6.0 to about 11.0, and b) at least one step of separation of impurities in a water—organic solvent system, followed by crystallization from the solution in methylene chloride, and wherein steps a) and b) are separated by steps of isolation of precipitate of olanzapine and can be accomplished in any order.Type: ApplicationFiled: January 22, 2008Publication date: June 3, 2010Applicant: TOMASZ KOZLUK NOBILUS ENTInventor: Tomasz Kozluk