Bicyclo Ring System Which Contains The Hetero Ring As One Of The Cyclos Patents (Class 540/593)
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Publication number: 20110136789Abstract: The present invention relates to compounds of formula I useful in the inhibition of c-Met protein kinase. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative disorders.Type: ApplicationFiled: March 31, 2010Publication date: June 9, 2011Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: David Lauffer, Pan Li, Nathan Waal, Kira Mcginty, Qing Tang, Steven Ronkin, Luc Farmer, Dean Shannon, Dylan Jacobs
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Patent number: 7956050Abstract: The compounds of the present invention are represented by the following aryl- and heteroaryl-substituted tetrahydrobenzazepine and dihydrobenzazapine derivatives having formulae I(A-E) and formula (II): where the carbon atom designated * is in the R or S configuration, and the substituents X and R1-R9 are as defined herein.Type: GrantFiled: July 17, 2006Date of Patent: June 7, 2011Assignee: Albany Molecular Research, Inc.Inventors: Bruce F. Molino, Shuang Liu, Aruna Sambandam, Peter R. Guzzo, Min Hu, Congxiang Zha, Kassoum Nacro, David D. Manning, Matthew L. Isherwood, Kristen N. Fleming, Wenge Cui, Richard E. Olson
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Publication number: 20110118235Abstract: Provided are compositions and methods useful for modulation of signaling through the Toll-like receptors TLR7 and/or TLR8. The compositions and methods have use in treating or preventing disease, including cancer, autoimmune disease, infectious disease, inflammatory disorder, graft rejection, and graft-verses-host disease.Type: ApplicationFiled: August 18, 2010Publication date: May 19, 2011Applicants: VentiRx Pharmaceuticals, Inc., Array BioPharma, Inc.Inventors: James Jeffry Howbert, Gregory Dietsch, Robert Hershberg, Laurence E. Burgess, George A. Doherty, C. Todd Eary, Robert D. Groneberg, Zachary Jones
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Publication number: 20110112072Abstract: 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: ApplicationFiled: January 12, 2011Publication date: May 12, 2011Inventors: L. Nathan Tumey, David C. Bom, Youssef L. Bennani, Michael J. Robarge
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Publication number: 20110112071Abstract: A compound represented by formula (I?): (wherein m, n, and p each represent 0 to 2; q represents 0 or 1; R1 represents halogen, a hydrocarbon group, a heterocyclic group, an alkoxy group, an alkoxycarbonyl group, a sulfamoyl group, a CN group, an NO2 group, or the like; R2 represents halogen, amino, a hydrocarbon group, an aromatic heterocyclic group, or an oxo group; X1 represents O, —NR3—, or —S(O)r-; X2 represents a methylene group, O, —NR3—, or —S(O)r-; Q? represents a heteroaryl group, a heteroarylalkyl group, a substituted aryl group, or an aralkyl group; Cycle moiety represents an aryl ring or a heteroaryl ring; and the wavy line represents an E-isomer or a Z-isomer), a salt of the compound, or a solvate of the compound or the salt. A pharmaceutical composition and a transient receptor potential type I (TRPV1) receptor antagonist each contain, as an active ingredient, at least one of the compound, a salt of the compound, and a solvate of the compound or the salt.Type: ApplicationFiled: January 18, 2011Publication date: May 12, 2011Applicant: MOCHIDA PHARMACEUTICAL CO., LTD.Inventors: Hideharu UCHIDA, Naoto Kosuga, Tsutomu Satoh, Daido Hotta, Tomoyuki Kamino, Yoshitaka Maeda, Ken-ichi Amano, Yasushige Akada
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Publication number: 20110092485Abstract: Provided are compositions and methods useful for modulation of signaling through the Toll-like receptors TLR7 and/or TLR8. The compositions and methods have use in treating or preventing disease, including cancer, autoimmune disease, infectious disease, inflammatory disorder, graft rejection, and graft-verses-host disease.Type: ApplicationFiled: August 18, 2010Publication date: April 21, 2011Applicants: VentiRx Pharmaceuticals, Inc., Array BioPharma, Inc.Inventors: James Jeffry Howbert, Gregory Dietsch, Robert Hershberg, Laurence E. Burgess, Joseph P. Lyssikatos, Brad Newhouse, Hong Woon Yang
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Publication number: 20110076214Abstract: One aspect of the present invention relates to salts that are room-temperature ionic liquids (RTILs), methods of making them, and methods of using them in connection with temporary or permanent gas sequestration. Another aspect of the present invention relates to a class of solvents which can be transformed into RTILs by exposure to a gas, and methods of using them in connection with temporary or permanent gas sequestration.Type: ApplicationFiled: January 28, 2008Publication date: March 31, 2011Applicant: Georgetown University Office of Technology commercializationInventors: Tao Yu, Richard G. Weiss, Taisuke Yamada, Mathew George
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Publication number: 20110071084Abstract: The present invention provides a benzazepine compound that can maintain for a long period of time the blood level of tolvaptan enabling to provide the desired pharmaceutical effects. The benzazepine compound of the present invention is represented by general formula (1) wherein R1 represents a —CO—(CH2)n—COR2 group (wherein n is an integer of 1 to 4, and R2 is (2-1) a hydroxy group; (2-2) a lower alkoxy group optionally substituted with a hydroxy group, a lower alkanoyl group, a lower alkanoyloxy group, a lower alkoxycarbonyloxy group, a cycloalkyloxycarbonyloxy group, or 5-methyl-2-oxo-1,3-dioxo-4-yl; or (2-3) an amino group optionally substituted with a hydroxy-lower alkyl group), or the like.Type: ApplicationFiled: June 26, 2008Publication date: March 24, 2011Inventors: Kazumi Kondo, Yasuhiro Menjo, Takahiro Tomoyasu, Shin Miyamura, Yuso Tomohira, Takakuni Matsuda, Keigo Yamada, Yusuke Kato
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CATALYSTS FOR METATHESIS REACTIONS INCLUDING ENANTIOSELECTIVE OLEFIN METATHESIS, AND RELATED METHODS
Publication number: 20110065915Abstract: The present invention provides compositions comprising metal complexes, and related methods. In some embodiments, metal complexes of the invention may be useful as catalysts for chemical reactions, including metathesis reactions, wherein the catalysts exhibit enhanced activity and stereoselectivity. In some embodiments, the invention may advantageously provide metal complexes comprising a stereogenic metal atom. Such metal complexes may be useful in enantioselective catalysis.Type: ApplicationFiled: January 23, 2009Publication date: March 17, 2011Applicant: TRUSTEES OF BOSTON COILEGEInventors: Steven J. Malcolmson, Amir H. Hoveyda, Simon J. Meek, Richard R. Schrock -
Publication number: 20110046114Abstract: The compounds of the present invention are represented by the following aryl- and heteroaryl-substituted tetrahydrobenzazepine and dihydrobenzazapine derivatives having formulae I(A-E) and formula (II): where the carbon atom designated * is in the R or S configuration, and the substituents X and R1-R9 are as defined herein.Type: ApplicationFiled: November 1, 2010Publication date: February 24, 2011Applicants: Albany Molecular Research, Inc., Bristol-Myers SquibbInventors: Bruce F. Molino, Shuang Liu, Aruna Sambandam, Peter R. Guzzo, Min Hu, Congxiang Zha, Kassoum Nacro, David D. Manning, Matthew L. Isherwood, Kristen N. Fleming, Wenge Cui, Richard E. Olson
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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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Publication number: 20110039827Abstract: This invention provides compounds of formula (I): wherein R1, R2, G, m, n, p and q have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.Type: ApplicationFiled: June 21, 2010Publication date: February 17, 2011Applicant: Millennium Pharmaceuticals, Inc.Inventors: Christopher Blackburn, Jeffrey P. Ciavarri, Kenneth M. Gigstad, He Xu
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Publication number: 20110040088Abstract: Certain fused pyrrole- and pyrazole-containing heterocyclic compounds are serotonin modulators useful in the treatment of serotonin-mediated diseases.Type: ApplicationFiled: October 25, 2010Publication date: February 17, 2011Inventors: Nicholas I. Carruthers, Wenying Chai, Xiaohu Deng, Curt A. Ovorak, Annette K. Kwok, Jimmiy T. Liang, Neelakandha Mani, Dale A. Rudolph, Victoria D. Wong
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Publication number: 20110021501Abstract: The invention relates to new piperidino-dihydrothienopyrimidines of formula 1, as well as pharmacologically acceptable salts thereof, wherein X is SO or SO2, but preferably SO, and wherein R1, R2, R3 and R4 may have the meanings given in claim 1, as well as pharmaceutical compositions which contain these compounds. These new piperidino-dihydrothienopyrimidines 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: January 27, 2011Applicant: 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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Patent number: 7875631Abstract: Compounds of the formula (I): where R2, R5, R6 have the meanings as given in the description, and U, V and W, respectively, may be CR2?, CR4? and CR6?, respectively (with the definitions of R2?, R4? and R6? again as in the description), or may be N, were synthesized. They were found to down-regulate or inhibit the expression or function of the IGF-1 receptor.Type: GrantFiled: March 12, 2004Date of Patent: January 25, 2011Assignee: Analytecon S.A.Inventors: Jan Gunzinger, Kurt Leander
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Publication number: 20110003795Abstract: The invention relates to substituted aromatic carboxamide and urea derivatives, to processes for the preparation thereof, to pharmaceutical compositions containing these compounds and also to the use of these compounds for preparing pharmaceutical compositions.Type: ApplicationFiled: May 6, 2010Publication date: January 6, 2011Applicant: Gruenenthal GmbHInventors: Robert FRANK, Gregor BAHRENBERG, Thomas CHRISTOPH, Klaus SCHIENE, Jean DE VRY, Nils DAMANN, Sven FRORMANN, Bernhard LESCH, Jeewoo LEE, Yong-Soo KIM, Myeong-Seop KIM
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Publication number: 20100331309Abstract: Compounds of a formula entitled, trans-4-[[(5S)-5-[[[3,5-bis(trifluoromethyl)phenyl]methyl](2-methyl-2H-tetrazol-5-yl)amino]-2,3,4,5-tetrahydro-7,9-dimethyl-1H-1-benzazepin-1-yl]methyl]-cyclohexanecarboxylic acid, as a free acid or a pharmaceutically acceptable salt thereof; and hydrates and other solvates in crystalline form; pharmaceutical formulations; and methods of use are disclosed.Type: ApplicationFiled: June 28, 2010Publication date: December 30, 2010Applicant: ELI LILLY AND COMPANYInventors: Xinchao Chen, Scott Alan Frank, David Michael Remick, Steven Wayne Pedersen
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Patent number: 7858613Abstract: The invention relates to substituted benzo-condensed cycloheptanone derivatives, to methods for producing them, to drugs containing said compounds and to the use of said compounds for producing drugs.Type: GrantFiled: May 17, 2006Date of Patent: December 28, 2010Assignee: Gruenenthal GmbHInventors: Claudia Hinze, Robert Frank, Ruth Jostock, Klaus Schiene, Michael Haurand, Hagen-Heinrich Hennies
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Publication number: 20100311721Abstract: The present invention encompasses compounds of general formula (1) wherein R1, R2 and R3 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and their use for preparing a pharmaceutical composition having the above-mentioned properties.Type: ApplicationFiled: March 4, 2008Publication date: December 9, 2010Applicant: Boehringer Ingelheim International GmbHInventors: Heinz Stadtmueller, Guido Boehmelt, Harald Engelhardt, Ulrich Hirt, Otmar Schaaf, Irene Waizenegger
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Publication number: 20100305100Abstract: 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: July 1, 2010Publication date: December 2, 2010Applicant: PTC THERAPEUTICS, INC.Inventors: Gary Mitchell Karp, Peter Seongwoo Hwang, James J. Takasugi, Hongyu Ren, Richard Gerald Wilde, Anthony Turpoff, Alexander Arefolov, Guangming Chen, Jeffrey Allen Campbell, Chunshi Li, Steven Paget, Nanjing Zhang, Xiaoyan Zhang, Jin Zhu
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Publication number: 20100273770Abstract: The present invention relates to novel oxadiazole derivatives having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders.Type: ApplicationFiled: December 19, 2008Publication date: October 28, 2010Inventors: Jag Paul Heer, Thomas Daniel Heightman, David Nigel Hurst, Christopher Norbert Johnson, John Skidmore, Ian David Wall
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Publication number: 20100273771Abstract: The present invention relates to novel oxadiazole derivatives having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders.Type: ApplicationFiled: December 19, 2008Publication date: October 28, 2010Inventors: Emmanuel Hubert Demont, Jag Paul Heer, John Skidmore, Ian David Wall, Jason Witherington, Thomas Daniel Heightman, David Nigel Hurst, Christopher Norbert Johnson
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Patent number: 7807664Abstract: A novel 4,4-difluoro-1,2,3,4-tetrahydro-5H-1-benzazepine derivative or a pharmaceutically acceptable salt thereof, which is useful as an agent for treating or preventing nocturia and/or diabetes insipidus, is provided.Type: GrantFiled: November 14, 2006Date of Patent: October 5, 2010Assignee: Astella Pharma Inc.Inventors: Hiroyuki Koshio, Issei Tsukamoto, Akio Kakefuda, Seijiro Akamatsu, Chikashi Saitoh
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Patent number: 7799824Abstract: Quaternary salt compounds of Formula (I) or pharmaceutically acceptable forms thereof, which are CCR2 antagonists and are useful in preventing, treating or ameliorating CCR2 mediated inflammatory syndromes, disorders or diseases in a subject in need thereof.Type: GrantFiled: June 22, 2005Date of Patent: September 21, 2010Assignee: OraPharma, Inc.Inventors: Bharat Lagu, Michael Wachter
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Publication number: 20100234454Abstract: The present invention relates to the use of vanilloid receptor (VR) antagonists, and more particularly vanilloid receptor 1 (VR1) antagonist, as analgesics in the treatment and/or prohylaxis of cnidaria envenomations.Type: ApplicationFiled: June 11, 2007Publication date: September 16, 2010Applicants: Katholieke Universiteit Leuven K.U. Leuven R&D, University of HawaiiInventors: Eva Cuypers, Evert Karlsson, Jan Tytgat, Angel Yanagihara
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Patent number: 7786108Abstract: Compounds of formula I wherein n, m, p, q, Y, R1 R2, R3a, R3b, R4, R5, and R6 are as defined herein and their pharmaceutical compositions and methods of use are disclosed.Type: GrantFiled: June 23, 2005Date of Patent: August 31, 2010Assignee: Eli Lilly and CompanyInventors: Xinchao Chen, Todd Fields, Nathan Bryan Mantlo, Xiaodong Wang
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Patent number: 7786105Abstract: The invention relates to pyrimidine compounds of general formula (I), and to the use of these compounds of general formula (I) and of the physiologically compatible acid addition salts of compounds (I) for producing a pharmaceutical agent for treating diseases, which respond to the influence of dopamine D3 receptor antagonists or agonists.Type: GrantFiled: June 3, 2005Date of Patent: August 31, 2010Assignee: Abbott GmbH & Co. KGInventors: Herve Geneste, Andreas Haupt, Wilfried Braje, Wilfried Lubisch, Gerd Steiner
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Publication number: 20100210624Abstract: The aryloxy- and heteroaryloxy-substituted tetrahydrobenzazepine derivative compounds of the present invention are represented by formulae (I) (A-E) having the following structure where the carbon atom designated * is in the R or S configuration and the substituents X and R1-R9 are as defined herein.Type: ApplicationFiled: May 8, 2008Publication date: August 19, 2010Applicants: ALBANY MOLECULAR RESEARCH, INC., BRISTOL-MYERS SQUIBB COMPANYInventors: Shuang Liu, Yuh-lin Allen Yang, Aruna Sambandam, Bruce F. Molino, Richard E. Olson
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Publication number: 20100204207Abstract: Compounds of Formula (I): wherein n, m, p, q, Y, R1, R2, R3a, R3b, R4, R5, and R6 are as defined herein and their pharmaceutical compositions and methods of use are disclosed.Type: ApplicationFiled: April 20, 2010Publication date: August 12, 2010Inventors: Xinchao Chen, Christopher Lawrence Cioffi, Sean Richard Dinn, Ana Maria Escribano, Maria Carmen Fernandez, Todd Fields, Robert Jason Herr, Nathan Bryan Mantlo, Eva Maria Martin De La Nava, Ana Isabel Mateo Herranz, Saravanan Parthasarathy, Xiaodong Wang
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Publication number: 20100190772Abstract: The present invention generally relates to compounds and pharmaceutical compositions containing the compounds. More specifically, compounds of the present invention are hexahydroazepinoindole and octahydroazepinoindole compounds. These compounds are serotonin receptor (5-HT) ligands and are useful for treating diseases, disorders, and conditions wherein modulation of the activity of serotonin receptors (5-HT) is desired (e.g. anxiety, depression and obesity).Type: ApplicationFiled: April 1, 2010Publication date: July 29, 2010Inventors: Youssef L. Bennani, Michael J. Robarge, David C. Bom, Norbert Varga, Lawrence N. Tumey
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Publication number: 20100184741Abstract: GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein R1a, R1b, R1c, R1d, R2, R2a, and A are as defined herein, including stereoisomers, esters, solvates, and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.Type: ApplicationFiled: April 4, 2008Publication date: July 22, 2010Inventors: Neil Ashweek, Mi Chen, Timothy Richard Coon, Todd Ewing, Wanlong Jiang, Willy Moree, Martin Rowbottom, Warren Wade, Liren Zhao, Yun-fei Zhu, Jinghua Yu, Graham Beaton
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Publication number: 20100173890Abstract: The present invention relates to new compounds of formula I, or salts, solvates or solvated salts thereof, process for their preparation and to new intermediates used in the preparation thereof, pharmaceutical compositions containing said compounds and to the use of said compounds in the treatment of 5-HT6 mediated disorders such as Alzheimer's disease, cognitive disorders, cognitive impairment associated with schizophrenia, obesity and Parkinson's disease.Type: ApplicationFiled: July 3, 2006Publication date: July 8, 2010Applicant: AstraZeneca ABInventors: Gunnar Nordvall, Fernando Sehgelmeble
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Publication number: 20100172867Abstract: The present invention relates to substituted 1H-pyrazolo-[3,4-d]pyrimidine-6-amine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted 1H-pyrazolo-[3,4-d]pyrimidine-6-amine 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: December 30, 2009Publication date: July 8, 2010Applicant: ArQule, Inc.Inventors: Syed M. Ali, Mark A. Ashwell, Jason Hill, Jean-Marc Lapierre, Magdi Moussa, Nivedita Namdev, Robert Nicewonger, Manish Tandon, Rui-Yang Yang
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Patent number: 7749992Abstract: Compounds of formula I wherein n, m, p, q, y, R1 R2, R3, R4, R5, and R6 are as defined herein and their pharmaceutical compositions and methods of use are disclosed as useful for treating artherosclerosis and its sequelae.Type: GrantFiled: October 7, 2004Date of Patent: July 6, 2010Assignee: Eli Lilly and CompanyInventors: Guoqing Cao, Ana Maria Escribano, Maria Carmen Fernandez, Todd Fields, Douglas Linn Gernert, Christopher Lawrence Cioffi, Robert Jason Herr, Nathan Bryan Mantlo, Eva Maria Martin De La Nava, Ana Isabel Mateo Herranz, Daniel Ray Mayhugh, Xiaodong Wang
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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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Patent number: 7718647Abstract: 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 hexahydroazepinoindole and octahydroazepinoindole compounds. These compounds are serotonin receptor (5-HT) ligands and are useful for treating diseases, disorders, and conditions wherein modulation of the activity of serotonin receptors (5-HT) is desired (e.g. anxiety, depression and obesity).Type: GrantFiled: June 29, 2005Date of Patent: May 18, 2010Assignee: Athersys, Inc.Inventors: Youssef L. Bennani, Michael J. Robarge, David C. Bom, Norbert Varga, Lawrence N. Tumey
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Publication number: 20100112090Abstract: [Purpose] The present invention provides compounds useful as agents for the prevention or treatment of a sex hormone-dependent disease or the like. [Solution] The present invention provides nitrogen-containing fused ring derivatives represented by the following general formula (I) which has a GnRH antagonistic activity, prodrugs, salts, pharmaceutical compositions containing the same, medicinal uses thereof and the like. In the formula (I), rings A and B are independently aryl or heteroaryl; RA and RB are independently halogen, cyano, alkyl, alkylsulfonyl, —OW1, —SW1, —COW2, —NW3W4, —SO2NW3W4, aryl, etc.; RC is H or alkyl; E is oxygen atom, etc.; U is single bond or alkylene; and X is Y, —CO—Y, —SO2—Y, —S-(alkylene)-Y, —O-(alkylene)-Y, —SO2-(alkylene)-Y, etc.; Y is Z or amino, etc.; and Z is cycloalkyl, heterocycloalkyl, aryl, heteroaryl, etc.Type: ApplicationFiled: April 16, 2008Publication date: May 6, 2010Applicant: KISSEI PHARMACEUTICAL CO., LTDInventors: Shigeru Yonekubo, Takashi Miyagi, Kohsuke Ohno, Mikie Kambara, Nobuhiko Fushimi
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Publication number: 20100113421Abstract: Compounds of Formula (I) are HIV reverse transcriptase inhibitors, wherein X, 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 or progression, 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: October 2, 2007Publication date: May 6, 2010Inventors: Theresa M. Williams, Xu-Fang Zhang, Vanessa E. Obligado, Rebecca A. Poehnelt
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Publication number: 20100105657Abstract: The present invention relates to new compounds of formula (I), or salts, solvates or solvated salts thereof, process for their preparation and to new intermediates used in the preparation thereof, pharmaceutical compositions containing said compounds and to the use of said compounds in the treatment of 5-HT6 mediated disorders such as Alzheimer's disease, cognitive disorders, cognitive impairment associated with schizophrenia, obesity and Parkinson's disease.Type: ApplicationFiled: July 3, 2006Publication date: April 29, 2010Applicant: AstraZeneca ABInventors: Gunnar Nordvall, Carl Petersson, Fernando Sehgelmeble
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Publication number: 20100099664Abstract: The object of the present invention is novel substituted pyrrolidine amides of the general formula (I) in which D, L. E, G, J, M, L1, L2, R4, and R5 are defined as in the specification, the tautomers, enantiomers, diastereomers, mixtures, and salts thereof, particularly physiologically tolerated salts with inorganic or organic acids or bases having valuable properties.Type: ApplicationFiled: March 26, 2008Publication date: April 22, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Kai Gerlach, Henning Priepke, Wolfgang Wienen, Annette Schuler-Metz, Georg Dahmann, Herbert Nar
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Publication number: 20100099663Abstract: The present invention is directed to a compound of formula I, wherein R1, R2, R3, X, A, m and n are as herein defined, the process for its preparation and its use thereof as a medicament.Type: ApplicationFiled: December 21, 2009Publication date: April 22, 2010Applicant: SANOFI-AVENTIS DEUTSCHLAND GMBHInventors: Manfred SCHUDOK, Armin HOFMEISTER
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Patent number: 7700583Abstract: A novel class of compounds of the general formula (I), their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds modulate the activity of 11?-hydroxy-steroid dehydrogenase type 1 (11?HSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, e.g. the metabolic syndrome.Type: GrantFiled: October 6, 2005Date of Patent: April 20, 2010Assignee: High Point Pharmaceuticals, LLCInventors: Anette Gundertofte, Anker Steen Jorgensen, Gita Camilla Tejlgaard Kampen, Henrik Sune Andersen, Inge Thoger Christensen, Kilburn Paul John
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Patent number: 7674787Abstract: The invention relates to conformationally constrained mimetics of Smac which function as inhibitors of Inhibitor of Apoptosis Proteins. The invention also relates to the use of these mimetics for inducing apoptotic cell death and for sensitizing cells to inducers of apoptosis.Type: GrantFiled: July 11, 2005Date of Patent: March 9, 2010Assignee: The Regents of the University of MichiganInventors: Shaomeng Wang, Haiying Sun, Zaneta Nikolovska-Coleska, Chao-Yie Yang, Liang Xu, Naoyuki G. Saito, Jianyong Chen
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Publication number: 20100048537Abstract: The present invention relates to a compound represented by formula [1] or a pharmaceutically acceptable salt thereof: In formula [1], one of X and Y is CH and the other is oxygen or sulfur; R is hydrogen, etc.; Z is hydrogen, etc.; Ar is phenyl, etc.; and n is 1 or 2 and or m is 1 or 2, excluding compounds where n is 2 and m is 2 simultaneously. Also provided is a pharmaceutical composition comprising a compound of formula [1] or a pharmaceutically acceptable salt thereof as an active ingredient. The composition is usable as an agent for the prevention or treatment of depression, panic disorder, anxiety, obsessive-compulsive disorder, chronic pain, fibromyalgia, obesity, stress urinary incontinence, and overactive bladder.Type: ApplicationFiled: March 28, 2008Publication date: February 25, 2010Applicant: Nippon Shinyaku Co., Ltd.Inventors: Masato Matsuoka, Tatsuya Oyama
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Publication number: 20100048829Abstract: The present invention relates to a liquid composition which comprises at least one polymer and at least one ionic liquid, the cations of which are derived from polycyclic amidine bases, and a process for isolating cellulose from cellulose-containing sources using at least one such ionic liquid.Type: ApplicationFiled: October 12, 2007Publication date: February 25, 2010Applicant: BASF AKTIENGESELLSCHAFTInventors: Giovanni D'Andola, Laszlo Szarvas, Klemens Massonne, Veit Stegmann
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Publication number: 20100022515Abstract: The invention provides compounds, pharmaceutical compositions comprising compound of following formula (I), and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of GPR119 (G protein-coupled receptor 119) such as obesity, diabetes and hyperlipidemia.Type: ApplicationFiled: January 22, 2008Publication date: January 28, 2010Applicant: IRM LLCInventors: Phillip B. Alper, Mihai D. Azimioara, Christopher Cow, Robert Epple, Songchun Jiang, Gerald Lelais, Pierre-Yves Michellys, Truc Ngoc Nguyen, Lucas Westcott-Baker, Baogen Wu
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Publication number: 20100022514Abstract: The invention relates to the use of compounds in the treatment of deacetylase-associated diseases and for the manufacture of pharmaceutical preparations for the treatment of said diseases.Type: ApplicationFiled: December 17, 2007Publication date: January 28, 2010Inventors: Young Shin Cho, Lei Jiang, Michael Shultz
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Publication number: 20090325900Abstract: The present invention provides a compound useful as an agent for the prevention or treatment of a sex hormone-dependent disease or the like. That is, the present invention provides a fused heterocyclic derivative represented by the following general formula (I), a pharmaceutical composition containing the same, a medicinal use thereof and the like. In the formula (I), ring A represents 5-membered cyclic unsaturated hydrocarbon or 5-membered heteroaryl; RA represents halogen, alkyl, alkenyl, alkynyl, carboxy, alkoxy, carbamoyl, alkylcarbamoyl or the like; ring B represents aryl or heteroaryl; RB represents halogen, alkyl, carboxy, alkoxy, carbamoyl, alkylcarbamoyl or the like; E1 and E2 represent an oxygen atom or the like; U represents a single bond or alkylene; X represents a group represented by Y, —SO2—Y, —O— (alkylene)-Y, —O-Z in which Y represents Z, amino or the like; Z represents cycloalkyl, heterocycloalkyl, aryl, heteroaryl or the like; or the like.Type: ApplicationFiled: October 17, 2006Publication date: December 31, 2009Applicant: KISSEI PHARMACEUTICAL CO., LTD.Inventors: Kohsuke Ohno, Takashi Miyagi, Tomonaga Ozawa, Nobuhiko Fushimi
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Patent number: 7598237Abstract: This invention provides progesterone receptor modulators having the structure: wherein R1 to R7, X, and Q are as defined in the specification; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: November 28, 2007Date of Patent: October 6, 2009Assignee: WyethInventors: Puwen Zhang, Jay Edward Wrobel, Eugene Anthony Terefenko, Jeffrey Curtis Kern
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Publication number: 20090227565Abstract: A compound of the formulae (I) or (II): wherein: Y is a moiety selected from NR or —(CH2)n; wherein R is hydrogen or (C1-C6) lower alkyl, and n is 1; represents: (1) a phenyl ring optionally substituted with one or two substituents selected, independently, from the group comprising hydrogen, (C1-C6) lower alkyl, halogen, cyano, CF3, hydroxy, (C1-C6) lower alkoxy, (C1-C6) lower alkoxy carbonyl, carboxy, —CONH2, —CONH[(C1-C6) lower alkyl], —CON[(C1-C6) lower alkyl]2; or (2) a 6-membered aromatic (unsaturated) heterocyclic ring having one nitrogen atom, optionally substituted by (C1-C6) lower alkyl, halogen or (C1-C6) lower alkoxy; represents: (1) a phenyl ring optionally substituted with one or two substituents selected, independently, from the group comprising hydrogen, (C1-C6) lower alkyl, halogen, cyano, CF3, hydroxy, (C1-C6) lower alkoxy, or (C1-C6) lower alkoxy carbonyl, carboxy, —CONH2, —CONH[(C1-C6) lower alkyl], —CON[(C1-C6) lower alkyl]2; or (2) a 5-membered aromatic (unsaturatType: ApplicationFiled: November 10, 2008Publication date: September 10, 2009Applicant: WYETHInventors: Amedeo A. FAILLI, John P. DUSZA, Thomas J. CAGGIANO, Jay S. SHUMSKY, Kevin A. MEMOLI, Eugene J. TRYBULSKI