Piperazine Ring Patents (Class 544/121)
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Publication number: 20090203696Abstract: Disclosed are compounds according to formula (I): wherein A, Q, X, Y, Z, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 are as defined herein. The disclosure also relates to pharmaceutical compositions containing a compound of formula (I), to processes for preparing the compounds of formula (I), and to methods of using the compounds of formula (I).Type: ApplicationFiled: December 15, 2008Publication date: August 13, 2009Applicant: SANOFI-AVENTISInventors: Jozsef Zsolt BOCSKEI, Gary MCCORT, Hans MATTER, Henning STEINHAGEN, Berangere THIERS
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Publication number: 20090203695Abstract: The present application relates to new compounds of formula (I), to pharmaceutical compositions comprising the compounds, to processes for their preparation, and to the use of the compounds as leptin receptor modulator mimetics in the preparation of medicaments against conditions associated with weight gain, type 2 diabetes and dyslipidemias.Type: ApplicationFiled: December 5, 2008Publication date: August 13, 2009Applicant: Biovitrum ABInventors: Michael Higginbottom, Viet-Anh Anne Horgan (nee Nguyen), Iain Simpson
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Publication number: 20090192160Abstract: The invention relates to compounds of formula (I) processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of conditions or disorders which are mediated via the GPR38 receptor.Type: ApplicationFiled: April 2, 2009Publication date: July 30, 2009Inventors: Darren Jason MITCHELL, Jonathan Thomas Seal, Mervyn Thompson, Susan Marie Westway, Samantha Louisa Brown
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Publication number: 20090192136Abstract: A compound of formula wherein the substituents are as described in the specification for the treatment of psychoses, pain, neurodegenerative disfunction in memory and learning, schizophrenia, dementia and other diseases in which cognitive processes are impaired, such as attention deficit disorders or Alzheimer's disease.Type: ApplicationFiled: July 22, 2008Publication date: July 30, 2009Inventors: Daniela Alberati-Giani, Synese Jolidon, Robert Narquizian, Matthias Heinrich Nettekoven, Roger David Norcross, Emmanuel Pinard, Henri Stalder
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Publication number: 20090181967Abstract: The present application relates to new compounds of formula (I), to pharmaceutical compositions comprising the compounds, to processes for their preparation, and to the use of the compounds as leptin receptor modulator mimetics in the preparation of medicaments against conditions associated with weight gain, type 2 diabetes and dyslipidemias.Type: ApplicationFiled: December 5, 2008Publication date: July 16, 2009Applicant: Biovitrum ABInventors: Joseph W. Boyd, Giles A. Brown, Michael Higginbottom
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Publication number: 20090182140Abstract: An alicyclic heterocyclic compound represented by the following formula or a pharmaceutically acceptable salt thereof: wherein ring A is a heterocyclic ring, ring B is a carbocyclic ring, a heterocyclic ring etc., P1 and P2 are CH or N, q and r are 0 to 2, X is —NH—, —O—, —CH2—, etc., Y is —CH2—, —CO—, —SO2—, etc., Z is —CO—, —SO2—, etc., and R3 is carbocyclic group, heterocyclic group, hydroxyl, alkoxy or amino, is useful as a controlling agent of the function of CCR4 useful for the prevention or treatment for bronchial asthma, atopic dermatitis, etc.Type: ApplicationFiled: November 30, 2006Publication date: July 16, 2009Applicant: MITSUBISHI TANABE PHARMA CORPORATIONInventors: Shigeru Furukubo, Hiroshi Miyazaki
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Patent number: 7560546Abstract: The present invention relates to compounds that are capable of inhibiting, modulating and/or regulating signal transduction of both receptor-type and non-receptor type tyrosine kinases. The compounds of the instant invention possess a core structure that comprises a sulfonyl indole moiety. The present invention is also related to the pharmaceutically acceptable salts, hydrates and stereoisomers of these compounds.Type: GrantFiled: August 5, 2003Date of Patent: July 14, 2009Assignee: Merck & Co., Inc.Inventors: Christopher J. Dinsmore, Douglas C. Beshore, Jeffrey M. Bergman, Craig W. Lindsley
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Publication number: 20090176763Abstract: The present invention relates to inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: ApplicationFiled: November 19, 2008Publication date: July 9, 2009Inventors: Francesco Salituro, Luc Farmer, Randy Bethiel, Edmund Harrington, Jeremy Green, John Court, Jon Come, David Lauffer, Alex Aronov, Hayley Binch, Dean Boyall, Jean-Damien Charrier, Simon Everitt, Damien Fraysse, Michael Mortimore, Francoise Pierard, Daniel Robinson, Jian Wang, Joanne Pinder, Tiansheng Wang, Albert Pierce
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Publication number: 20090170836Abstract: This invention comprises the novel compounds of formula (I) wherein n, t, R1, R2, R3, R4, L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.Type: ApplicationFiled: February 18, 2009Publication date: July 2, 2009Inventors: Patrick Rene Angibaud, Isabelle Noelle Constance Pilatte, Sven Franciscus Anna Van Brandt, Bruno Roux, Peter Ten Holte, Marc Gustaaf Celine Verdonck, Lieven Meerpoel, Alexey Borisovich Dyatkin
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Publication number: 20090163708Abstract: This invention relates to a method of preparing mesylate salts of compounds that inhibit IL-12, IL-23 and/or IL-27 production.Type: ApplicationFiled: April 26, 2008Publication date: June 25, 2009Applicant: Synta Pharmaceuticals Corp.Inventors: Elena Kostik, Lijun Sun, Keizo Koya, Pierre L. Boulas
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Patent number: 7550462Abstract: Compounds of formula (I) wherein R1 is 2-indanyl, R2 is 1-methylpropyl, R3 is a group selected from 2,6-dimethyl-3-pyridyl or 4,6-dimethyl-3-pyridyl, R4 represents methyl and R5 represents hydrogen or methyl or, R4 and R5 together with the nitrogen atom to which they are attached represent morpholino and pharmaceutically acceptable derivatives thereof are described, as are processes for their preparation, pharmaceutical compositions containing them and their use in medicine, particularly their use as oxytocin antagonists.Type: GrantFiled: June 21, 2005Date of Patent: June 23, 2009Assignee: Glaxo Group LimitedInventors: Alan David Borthwick, Deirdre Mary Bernadette Hickey, John Liddle, Andrew McMurtrie Mason
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Publication number: 20090156589Abstract: A compound represented by the following general formula (1) or (100), a salt thereof or a hydrate of the foregoing has excellent cell adhesion inhibitory action and cell infiltration inhibitory action. wherein R10 represents 5- to 10-membered cycloalkyl etc. optionally substituted with hydroxyl etc., R30, R31 and R32 may be the same or different and each represents hydrogen etc., R40 represents C1-10 alkyl etc. optionally substituted with hydroxyl etc., n represents an integer of 0, 1 or 2, X1 represents CH or nitrogen, and R20, R21, R22 and R23 may be the same or different and each represents hydrogen etc.Type: ApplicationFiled: June 14, 2006Publication date: June 18, 2009Applicant: EISAI R&D MANAGEMENT CO., LTD.Inventors: Tetsuya Kawahara, Makoto Kotake, Naoki Yoneda, Shinsuke Hirota, Masayoshi Ohkuro
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Publication number: 20090149447Abstract: Muscarinic Acetylcholine receptor antagonists and methods of using them are provided.Type: ApplicationFiled: November 15, 2005Publication date: June 11, 2009Applicant: GLAXO GROUP LIMITEDInventors: Brian W. Budzik, Anthony W.J. Cooper, Jian Jin, Dramane I. Laine, Brent W. McCleland, Michael R. Palovich, Ralph A. Rivero, Yonghui Wang, Haibo Xie, Chongjie Zhu
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Patent number: 7544683Abstract: The present invention relates to compounds of formula I wherein R1 and R2 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.Type: GrantFiled: June 10, 2008Date of Patent: June 9, 2009Assignee: Hoffmann-La Roche Inc.Inventors: Delphine Gaufreteau, Matthias Nettekoven, Jean-Marc Plancher, Olivier Roche, Sebastien Schmitt, Tadakatsu Takahashi
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Publication number: 20090143575Abstract: Therapeutic benzimidazoles and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, duodenal ulcers,Type: ApplicationFiled: February 6, 2009Publication date: June 4, 2009Inventors: Chenera Balan, Yunxin Bo, Celia Dominguez, Christopher H. Fotsch, Vijay K. Gore, Vu Van Ma, Mark H. Norman, Vassil I. Ognyanov, Yi-xin Qian, Xianghong Wang, Ning Xi, Shimin Xu
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Publication number: 20090143364Abstract: and the pharmaceutically acceptable salts and esters thereof, wherein X1, X2, X3, Y1, Y2 and R are described herein inhibit the interaction of MDM2 protein with a p53-like peptide and hence have anti proliferative activity.Type: ApplicationFiled: February 5, 2009Publication date: June 4, 2009Inventors: Nader Fotouhi, Gregory Jay Haley, Klaus B. Simonsen, Binh Thanh Vu, Stephen Evan Webber
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Patent number: 7541359Abstract: Certain N-heteroarylpiperazinyl urea compounds of Formula (I), as defined in the specification, are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity. Thus, the compounds may be administered to treat, e.g., anxiety, pain, inflammation, sleep disorders, eating disorders, or movement disorders (such as multiple sclerosis).Type: GrantFiled: June 28, 2006Date of Patent: June 2, 2009Assignee: Janssen Pharmaceutica N.V.Inventors: Richard Apodaca, J. Guy Breitenbucher, Kanaka Pattabiraman, Mark Seierstad, Wei Xiao
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Publication number: 20090137396Abstract: The present invention relates to the use of piperazine compounds of the formula I or of the agriculturally useful salts of piperazine compounds of the formula I as herbicides, where in formula I the variables are as defined in the claims and the description. Moreover, the invention relates to compositions comprising, in addition to auxiliaries customary for formulating crop protection agents, piperazine compounds of the formula I or agriculturally useful salts of I, and to a process for preparing these compositions. Furthermore, the invention relates to certain piperazine compounds of the formula I, a process for preparing piperazine compounds of the formula I and a method for controlling unwanted vegetation which comprises treating plants, their seeds and/or their habitat with at least one piperazine compound of the formula I.Type: ApplicationFiled: January 4, 2007Publication date: May 28, 2009Applicant: BASF SEInventors: Eike Hupe, Cyrill Zagar, Matthias Witschel, Toralf Kuehn, William Karl Moberg, Liliana Parra Rapado, Frank Stelzer, Andrea Vescovi, Robert Reinhard, Bernd Sievernich, Klaus Grossmann, Thomas Ehrhardt
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Publication number: 20090131436Abstract: Novel pyrimidine derivatives of formula (I) to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them.Type: ApplicationFiled: August 26, 2005Publication date: May 21, 2009Inventors: Patricia Imbach, Eiji Kawahara, Kazuhide Konishi, Naoko Matsuura, Takahiro Miyake, Osamu Ohmori, Johannes Roesel, Naoki Teno, Ichiro Umemura
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Publication number: 20090130117Abstract: The present invention provides tetrazole compounds, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising the tetrazole compounds. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a compound of the present invention.Type: ApplicationFiled: October 14, 2008Publication date: May 21, 2009Applicant: ARQULE, INC.Inventors: Rui-Yang Yang, Syed M. Ali, Mark A. Ashwell, Eugene Kelleher, Rocio Palma, Neil Westlund
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Patent number: 7534788Abstract: The present invention relates to compounds of formula I wherein X, A and R1 to R4 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.Type: GrantFiled: July 16, 2008Date of Patent: May 19, 2009Assignee: Hoffmann-La Roche Inc.Inventors: Peter Mohr, Matthias Nettekoven, Jean-Marc Plancher, Hans Richter, Olivier Roche, Tadakatsu Takahashi, Sven Taylor
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Publication number: 20090124620Abstract: The present invention relates to an inhibitor of plasminogen activator inhibitor-1. The present invention further relates to a pharmaceutical composition that has an inhibitory action on PAI-1 activity and is useful in the prevention and treatment of various diseases whose onset is associated with PAI-1 activity. Furthermore, the present invention relates to a novel compound having PAI-1 inhibitory activity represented by the following general formula (I), and a salt thereof. Each symbol is defined as those in the specification.Type: ApplicationFiled: March 12, 2008Publication date: May 14, 2009Inventors: Toshio Miyata, Nagahisa Yamaoka, Hidehiko Kodama
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Publication number: 20090118284Abstract: Disclosed are the ERK inhibitors of formula 1.0: and the pharmaceutically acceptable salts, esters and solvates thereof. Q is a piperidine or piperazine ring that can have a bridge or a fused ring. The piperidine ring can have a double bond in the ring. All other substitutents are as defined herein. Also disclosed are methods of treating cancer using the compounds of formula 1.0.Type: ApplicationFiled: June 5, 2007Publication date: May 7, 2009Inventors: Alan B. Cooper, Yongqi Deng, Gerald W. Shipps, JR., Neng-Yang Shih, Hugh Y. Zhu, Robert Sun, Joseph M. Kelly, Ronald J. Doll, Yang Nan, Tong Wang, Jagdish A. Desai, James J-S Wang, Youhao Dong, Vincent S. Madison, Li Xiao, Alan W. Hruza, M. Arshad Siddiqui, Ahmed A. Samatar, Sunil Paliwal, Hon-Chung Tsui, Azim Alan Celebi, Yiji Wu, Sobhana Babu Boga, Abdul-Basit Alhassan, Xiaolei Gao, Liang Zhu, Mehul Patel
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Patent number: 7528135Abstract: The present invention relates to compounds of formula I wherein R1, R2 and A are as defined in the description and claims, and pharmaceutically acceptable salts thereof as well as to pharmaceutical composition comprising these compounds and to methods for their preparation. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.Type: GrantFiled: November 30, 2005Date of Patent: May 5, 2009Assignee: Hoffmann-La Roche Inc.Inventors: Matthias Heinrich Nettekoven, Olivier Roche, Rosa Maria Rodriguez-Sarmiento
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Publication number: 20090111789Abstract: There are provided compounds of the formula or the pharmaceutically acceptable salts thereof, wherein X, Y, Z, V1, V2, R1, R2, R3, R4 and R5 are herein described. These compounds are useful as anticancer agents.Type: ApplicationFiled: October 9, 2008Publication date: April 30, 2009Inventors: David Joseph Bartkovitz, Jianping Cai, Xin-Jie Chu, Hongju Li, Allen John Lovey, Binh Thanh Vu, Chunlin Zhao
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Patent number: 7524845Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.Type: GrantFiled: June 22, 2006Date of Patent: April 28, 2009Assignee: ChemoCentryx, Inc.Inventors: Penglie Zhang, Andrew M. K. Pennell, John J. Kim Wright, Wei Chen, Manmohan R. Leleti, Yandong Li, Lianfa Li, Yuan Xu
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Publication number: 20090105251Abstract: Compounds, pharmaceutical compositions, kits and methods are provided for use with renin that comprise a compound selected from the group consisting of: wherein the variables are as defined herein.Type: ApplicationFiled: December 10, 2007Publication date: April 23, 2009Inventors: Benjamin Jones, Andrey A. Kiryanov, Stephen W. Kaldor
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Publication number: 20090105209Abstract: This application discloses pyridine and pyrimidine compounds according to formula I wherein R1, R2, R3, R4, R5, X1 and A are as described herein which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of formula I and at least one carrier, diluent or excipient.Type: ApplicationFiled: October 23, 2008Publication date: April 23, 2009Inventors: Nolan James Dewdney, Rama K. Kondru, Yan Lou, Michael Soth, Tobias Gabriel
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Publication number: 20090099156Abstract: Compounds of formula (I) Q-L-W—C(?X)-Z-P wherein Q is an amine of the formula —N(R1)(R2); L is an alkyl or heterocyclyl-alkyl linker; W is a 6- or 7-membered aliphatic ring comprising ring atoms Y1 and Y2 which are linked to groups L and C(X) respectively and Y1 and Y2 are independently selected from N and C; X is O, N, N—CN or S; Z is NR3; P is an optionally substituted monocyclic or bicyclic aryl or heteroaryl group; and pharmaceutically acceptable salts or solvates thereof, are useful in the treatment of C-C chemokine mediated conditions.Type: ApplicationFiled: December 19, 2005Publication date: April 16, 2009Inventors: Justin Fairfield Bower, Jeffrey Philip Poyser, Paul Turner, David Waterson, Jon Winter
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Publication number: 20090093455Abstract: The present invention provides novel quinolone compounds and pharmaceutical composition thereof which may inhibit cell proliferation and/or induce cell apoptosis. The present invention also provides methods of preparing such compounds and compositions, and methods of making and using the same.Type: ApplicationFiled: October 3, 2008Publication date: April 9, 2009Inventors: Johnny Yasuo NAGASAWA, Fabrice PIERRE, Mustapha HADDACH, Michael SCHWAEBE, Levan DARJANIA, Jeffrey P. WHITTEN
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Patent number: 7514436Abstract: Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I): where x, y, W, V, R2, R3, R4, R5, R6, R6a, R7, R7a, R8, R8a, R9 and R9a are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.Type: GrantFiled: July 29, 2004Date of Patent: April 7, 2009Assignee: Xenon Pharmaceuticals Inc.Inventors: Heinz W. Gschwend, Vishnumurthy Kodumuru, Shifeng Liu, Rajender Kamboj
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Patent number: 7514433Abstract: The present invention relates to the compounds of formula I: wherein R1 to R4 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.Type: GrantFiled: July 19, 2007Date of Patent: April 7, 2009Assignee: Hoffmann-La Roche Inc.Inventors: Matthias Nettekoven, Olivier Roche
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Publication number: 20090082330Abstract: Compounds of Formula I that inhibit Btk are described herein. Pharmaceutical compositions comprising at least one compound of Formula I, together with at least one pharmaceutically acceptable vehicle chosen from carriers, adjuvants, and excipients, are described. Methods of treating patients suffering from certain diseases responsive to inhibition of Btk activity and/or B-cell activity are described. Methods for determining the presence of Btk in a sample are described.Type: ApplicationFiled: September 19, 2008Publication date: March 26, 2009Inventors: Peter A. BLOMGREN, Kevin S. Currie, Seung H. Lee, Scott A. Mitchell, Jianjun Xu, Aaron C. Schmitt, Zhongdong Zhao, Pavel E. Zhichkin, Douglas G. Stafford, Jeffrey E. Kropf
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Patent number: 7507732Abstract: 6,7-Dihydro-5H-cyclopenta[b]pyridine and 5,6,7,8-tetrahydroquinoline compounds of Formula (I), including salts, hydrates and solvates thereof, that act as 5-HT2 receptor ligands and their uses in the treatment of diseases linked to the activation of 5-HT2c receptors are described herein.Type: GrantFiled: March 31, 2006Date of Patent: March 24, 2009Assignee: Pfizer Inc.Inventors: Bruce A. Lefker, Kevin K. -C. Liu, Hou Chen, Steven Blair Coffey
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Patent number: 7507736Abstract: The present invention relates to compounds of formula I wherein A and R1 to R4 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.Type: GrantFiled: January 25, 2008Date of Patent: March 24, 2009Assignee: Hoffmann-La Roche Inc.Inventors: Matthias Nettekoven, Jean-Marc Plancher, Hans Richter, Olivier Roche, Sven Taylor
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Publication number: 20090076006Abstract: The present invention relates to HSP90 inhibitors containing a zinc binding moiety and their use in the treatment of cell proliferative diseases such as cancer. The said derivatives may further act as HDAC inhibitors.Type: ApplicationFiled: September 10, 2008Publication date: March 19, 2009Inventors: Changgeng Qian, Xiong Cai, Haixiao Zhai
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Publication number: 20090069305Abstract: The present invention relates to substituted nitrogen-containing heteroaryl derivatives, pharmaceutical compositions containing them, and methods of using any of these derivatives and compositions for H4 receptor activity modulation and the treatment of states mediated by histamine H4 receptor activity.Type: ApplicationFiled: September 11, 2008Publication date: March 12, 2009Inventors: Michael D. Gaul, Bao-Ping Zhao, Xizhen Zhu
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Publication number: 20090054392Abstract: The present invention relates to naphthylpyrimidine analogs, methods of making naphthylpyrimidine analogs, compositions comprising a naphthylpyrimidine analog, and methods for treating canonical Wnt-?-catenin cellular messaging system-related disorders comprising administering to a subject in need thereof an effective amount of a naphthylpyrimidine, naphthylpyrazine and naphthylpyridazine analog.Type: ApplicationFiled: August 19, 2008Publication date: February 26, 2009Applicant: WyethInventors: Jeffrey Claude Pelletier, Luciana de Araujo Felix, Daniel Michael Green, Diane Barbara Hauze, Joseph Theodore Lundquist, IV, Charles William Mann, John Francis Mehlmann, John Francis Rogers, JR., Matthew Douglas Vera, Albert John Molinari
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Patent number: 7494994Abstract: A compound selected from those of formula (I): wherein: X represents a C(O) or SO2 group, R1 represents an aryl group or a group NR3R4 wherein R3 and R4 are as defined in the description, R2 represents an alkyl, (C3-C8)cycloalkyl or (C3-C8)cycloalkyl-(C1-C6)alkyl group, its isomers, and addition salts thereof, and medicinal products containing the same which are useful in treating conditions treatable by antagonists of type H3 central histamine receptors.Type: GrantFiled: May 11, 2006Date of Patent: February 24, 2009Assignee: Les Laboratoires ServierInventors: Patrice Desos, Alexis Cordi, Pierre Lestage
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Patent number: 7494995Abstract: A compound selected from those of formula (I): wherein: R1 represents an NR3SO2R4 group wherein: R3 represents a hydrogen atom or an alkyl group, R4 represents an alkyl group, aryl group or NR5R6 group, R2 represents an alkyl, cycloalkyl or cycloalkylalkyl group, and medicinal products containing the same which are useful in treating conditions treatable by antagonists of type H3 central histamine receptors.Type: GrantFiled: May 11, 2006Date of Patent: February 24, 2009Assignee: Les Laboratoires ServierInventors: Patrice Desos, Alexis Cordi, Pierre Lestage
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Patent number: 7491821Abstract: Compounds of formula 1 are modulators of P2X3 useful for the treatment of pain and genitourinary, gastrointestinal, and respiratory disorders: wherein R1 is —C(?S)CH3, pyridyl, pyrimidinyl, pyrazinyl, thiazolyl, furyl, furylcarbonyl, acetyl, or carbamoyl; R2a and R2b are independently H, methyl, or ethyl; R3 is H or methyl; Y is a bond, —(CR4R5)n— or —CR4?CR5—; wherein R4 and R5 are each independently H or methyl and n is 1 or 2; X is N or CH; A is phenyl, 5-membered heterocyclyl, or 6-membered heterocyclyl; R6, R7 and R8 are each independently H, halo, lower alkyl, cycloalkyl, alkylthio, alkylthio-lower alkyl, alkylsulfonyl-lower alkyl, di(lower alkyl)amino-lower alkyl, morpholinyl-lower alkyl, 4-methyl-piperazinyl-methyl, trifluoromethyl, pyridyl, tetrazolyl, thiophenyl, phenyl, biphenyl, or benzyl (where thiophenyl, phenyl and benzyl are substituted with 0-3 lower alkyl, halo, sulfonamido, trifluoromethyl, lower alkoxy or lower alkylthio) or R6 and R7 together form a 5-membered or 6-membered carbocyclType: GrantFiled: August 11, 2006Date of Patent: February 17, 2009Assignee: Roche Palo Alto LLCInventors: Christine E. Brotherton-Pleiss, Michael Patrick Dillon, Shelley K. Gleason, Clara Jeou Jen Lin, Ryan Craig Schoenfeld, Marzia Villa, Yansheng Zhai
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Publication number: 20090042865Abstract: A compound of formula I: wherein: R1 and R2 are independently selected from hydrogen, an optionally substituted C1-7 alkyl group, C3-20 heterocyclyl group, or C5-20 aryl group, or may together form, along with the nitrogen atom to which they are attached, an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; X is CH or N; n is 1 or 2; RC1 and RC2 are independently selected from H and methyl; when X is N, RX is selected from the group consisting of H, and optionally substituted C1-7 alkyl, C3-20 heterocyclyl, C5-20 aryl, acyl, ester, amido and sulfonyl; and when X is CH, RX is selected from the group consisting of H, and optionally substituted C1-7 alkyl, C3-20 heterocyclyl, C5-20 aryl, acyl, ester, amido, sulfonyl, amino and ether.Type: ApplicationFiled: July 18, 2008Publication date: February 12, 2009Inventors: Mark Frigerio, Marc Geoffrey Hummersone, Keith Allan Menear, Christine Sarah Bailey, Heather Mary Ellen Duggan, Sylvie Gomez, Niall Morrison Barr Martin
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Publication number: 20090043091Abstract: A compound of formula I: and isomers, salts, solvates, chemically protected forms, and prodrugs thereof, wherein: R1 and R2 together form, along with the nitrogen atom to which they are attached, an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; and RN1 is selected from hydrogen, an optionally substituted C1-7 alkyl group, an optionally substituted C3-20 heterocyclyl group, an optionally substituted C5-20 aryl group, an acyl group, an ester group and an amido group, and its use as a pharmaceutical.Type: ApplicationFiled: September 19, 2008Publication date: February 12, 2009Applicant: KUDOS PHARMACEUTICALS LIMITEDInventors: Graeme Cameron Murray Smith, Niall Morrison Barr Martin, Xiao-Ling Fan Cockcroft, Ian Timothy Williams Matthews, Keith Allan Menear, Laurent Jean Martin Rigoreau, Marc Geoffrey Hummersone, Roger John Griffin
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Publication number: 20090036443Abstract: The present invention relates to thienopyrrole compounds of formula (I); wherein A, B, Y, Ar, n, Z and X1 are as defined herein, and pharmaceutically acceptable salts thereof, useful in the prevention and treatment of hepatitis C infections.Type: ApplicationFiled: September 7, 2004Publication date: February 5, 2009Inventors: Barbara Attenni, Jose Ignacio Martin Hernando, Savina Malancona, Frank Narjes, Jesus Maria Ontoria Ontaria, Michael Rowley
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Patent number: 7479559Abstract: The present invention relates to novel benzyl(idene)-lactam derivatives, compounds of the formula I wherein R1 is a group of the formula G1 or G2 depicted below, wherein R1, R3, R6, R13 X, a, n and m are as defined herein, their pharmaceutically acceptable salts, and pharmaceutical compositions which include selective antagonists, inverse agonists and partial agonists of serotonin 1 (5-HT1) receptors, specifically, of one or both of the 5-HT1A and 5-HT1B receptors. The compounds of the invention are useful in treating or preventing depression, anxiety, obsessive compulsive disorder (OCD) and other disorders for which a 5-HT1 agonist or antagonist is indicated and have reduced potential for cardiac side effects, in particular QTc prolongation.Type: GrantFiled: March 17, 2005Date of Patent: January 20, 2009Assignee: Pfizer Inc.Inventors: Michael Aaron Brodney, Stephane Caron, Christopher John Helal, Jeffrey W. Raggon, Yong Tao, Nga M. Do
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Publication number: 20090018118Abstract: The invention is related to novel substituted diazaheterocycles useful as effective antihypercholesterolemic agents, methods of their preparation, and pharmaceutical compositions containing them.Type: ApplicationFiled: December 27, 2006Publication date: January 15, 2009Inventors: Uros Urleb, Darko Kocjan, Tina Korosec, Damjana Rozman, Jure Acimovic, Alenka Tomazic, Breda Rode
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Publication number: 20090004106Abstract: The present invention provides novel radioligands for the 5-HT1B receptor of the formula I.Type: ApplicationFiled: February 14, 2007Publication date: January 1, 2009Inventors: John Richard Heys, Edward Pierson, William Potts
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Publication number: 20090005375Abstract: The present invention relates to acetyl coenzyme-A carboxylase (“ACC”) inhibiting compounds of the formula wherein the variables are as defined herein. In particular, the present invention relates to ACC1 and/or ACC2 inhibitors, compositions of matter, kits and articles of manufacture comprising these compounds, methods for inhibiting ACC1 and/or ACC2, and methods of making the inhibitors.Type: ApplicationFiled: March 21, 2008Publication date: January 1, 2009Inventors: Edcon Chang, Matthew H. McNeill
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Publication number: 20090005380Abstract: The present invention relates to compounds of formula I wherein R1 and R2 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.Type: ApplicationFiled: June 10, 2008Publication date: January 1, 2009Inventors: Delphine Gaufreteau, Matthias Nettekoven, Jean-Marc Plancher, Olivier Roche, Sebastien Schmitt, Tadakatsu Takahashi
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Publication number: 20080318948Abstract: The present invention provides compounds of the formula which are activators of glucokinase activity and, thus, may be employed as therapeutic agents for the treatment of glucokinase mediated conditions. Accordingly, the compounds of formula (I) may be employed for the prevention and the treatment of impaired glucose tolerance, type 2 diabetes and obesity.Type: ApplicationFiled: September 28, 2006Publication date: December 25, 2008Inventor: Gregory Raymond Bebernitz