Chalcogen Hetero Ring Attached Directly Or Indirectly To The Piperazine Ring By Nonionic Bonding Patents (Class 514/253.11)
-
Patent number: 7816352Abstract: The present invention provides compounds that act as selective agents to protect against unintentional cell death or tissue damage and can relieve side effects of cancer treatment such as, for example, oral mucositis, hair loss, diarrhea due to damage to the gastrointestinal epithelium, and myelosuppression. In addition, these compounds can be used to prevent premature cell death when the cell death is caused by signals from damaged cells, for example, signals generated as the result of a traumatic incident or an ischemic episode.Type: GrantFiled: March 10, 2006Date of Patent: October 19, 2010Assignee: The Regents of The University of CaliforniaInventors: Dennis A. Carson, Howard B. Cottam, Sylvie Barchéchath, Mary Patricia Corr
-
Publication number: 20100249089Abstract: The present invention relates to a breast cancer resistance protein (BCRP/ABCG2) inhibitor. The invention provides an acrylonitrile derivative represented by formula (1): (wherein A represents an optionally substituted 3- to 8-membered heterocyclic ring) or a salt thereof.Type: ApplicationFiled: December 2, 2008Publication date: September 30, 2010Applicant: KABUSHIKI KAISHA YAKULT HONSHAInventors: Ryuta Yamazaki, Hiroshi Hatano, Takashi Yaegashi, Yoshiaki Igarashi, Oh Yoshida, Yoshikazu Sugimoto
-
Publication number: 20100215661Abstract: Compounds of formula (I): are inhibitors of p38 kinase and are useful in the treatment of conditions or disease states mediated by p38 kinase activity or mediated by cytokines produced by the activity of p38.Type: ApplicationFiled: February 26, 2010Publication date: August 26, 2010Inventors: Nicola Mary ASTON, Paul Bamborough, Ann Louise Walker
-
Publication number: 20100210633Abstract: Chemokine receptor antagonists, in particular, compounds of Formula (I) that act as antagonists of the chemokine CCR2 receptor, including pharmaceutical compositions and uses thereof to treat or prevent diseases associated with monocyte accumulation, lymphocyte accumulation or leukocyte accumulation are described herein.Type: ApplicationFiled: October 12, 2007Publication date: August 19, 2010Applicant: EPIX Delaware, Inc.Inventors: Jian Lin, Dongli Chen, Steffi Koerner, Rosa E. Melendez, Pradyumma Mohanty, Efrat Ben-Zeev, Merav Fichman, Yael Marantz, Oren Becker, Dilara McCauley, Pini Orbach, Ashis K. Saha, Sharon Shacham, Michael Xie
-
Publication number: 20100210661Abstract: An object of the present invention is to provide a STAT3/5 activation inhibitor. The present invention provides a STAT3/5 activation inhibitor containing an aromatic compound represented by the general formula or a salt thereof as an active ingredient: wherein X1 represents a nitrogen atom or a group —CH?, R1 represents a group —Z—R6, in which Z represents a group —CO—, a group —CH(OH)— or the like, R6 represents a 5- to 15-membered monocyclic, dicyclic or tricyclic saturated or unsaturated heterocyclic group having 1 to 4 nitrogen atoms, oxygen atoms or sulfur atoms, R2 represents a hydrogen atom or a halogen atom, Y represents a group —O—, a group —CO—, a group —CH(OH)— or a lower alkylene group, and A represents a group wherein R3 represents a hydrogen atom, a lower alkoxy group or the like, p represents 1 or 2, R4 represents an imidazolyl lower alkyl group or the like.Type: ApplicationFiled: October 2, 2007Publication date: August 19, 2010Applicant: OTSUKA PHARMACEUTICAL CO., LTD.Inventors: Kazuo Sekiguchi, Takashi Suzuki, Yutaka Ohbuchi, Mitsuhiro Okuno, Naoto Ohi, Kenji Ohnishi, Masaaki Motoyama, Kenji Yoshida, Takeshi Kodama, Kazuhisa Sugiyama, Seiji Akamatsu, Kunihiko Kiyono, Yasuo Yanagihara, Takashi Watanabe, Kazuhiko Hayashi, Hideo Tanaka, Takumi Sumida
-
Publication number: 20100210638Abstract: Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.Type: ApplicationFiled: April 28, 2010Publication date: August 19, 2010Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Sara S. Hadida Ruah, Matthew Hamilton, Mark Miller, Peter D.J. Grootenhuis, Brian Bear, Jason McCartney, Jinglan Zhou
-
Patent number: 7776862Abstract: The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of said compound, or of said prodrug, said compound having the general structure shown in Formula 1: and the pharmaceutically acceptable salts, solvates and esters thereof. Also disclosed is a method of treating chemokine mediated diseases, such as, palliative therapy, curative therapy, prophylactic therapy of certain diseases and conditions such as inflammatory diseases (non-limiting example(s) include, psoriasis), autoimmune diseases (non-limiting example(s) include, rheumatoid arthritis, multiple sclerosis), graft rejection (non-limiting example(s) include, allograft rejection, xenograft rejection), infectious diseases (e.Type: GrantFiled: February 14, 2006Date of Patent: August 17, 2010Assignee: Schering CorporationInventors: Brian F. McGuinness, Stuart B. Rosenblum, Joseph A. Kozlowski, Gopinadhan N. Anilkumar, Seong Heon Kim, Neng-Yang Shih, Chung-Her Jenh, Paul J. Zavodny, Douglas W. Hobbs, Guizhen Dong, Yuefei Shao, Lisa Guise Zawacki, Cangmeng Yang, Carolyn Dilanni Carroll
-
Publication number: 20100203039Abstract: The present invention is directed to compounds of Formula I: which are modulators of chemokine receptors. The compounds of the invention, and compositions thereof, are useful in the treatment of diseases related to chemokine receptor expression and/or activity.Type: ApplicationFiled: April 16, 2010Publication date: August 12, 2010Inventor: Chu-Biao Xue
-
Publication number: 20100184766Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.Type: ApplicationFiled: January 18, 2010Publication date: July 22, 2010Applicant: ABBOTT LABORATORIESInventors: Aaron R. Kunzer, Steven W. Elmore, Laura A. Hexamer, Cheol-Min Park, Andrew J. Souers, Gerard M. Sullivan, Gary T. Wang, Xilu Wang, Michael D. Wendt
-
Patent number: 7754719Abstract: Compound of the formula (I) wherein R1, R2, n and m are as defined in the specification. The compounds of formula (I) are somatostatin sst1 receptor antagonists.Type: GrantFiled: July 13, 2006Date of Patent: July 13, 2010Assignee: Novartis AGInventors: Daniel Hoyer, Konstanze Hurth, Thomas J. Troxler
-
Patent number: 7754721Abstract: Compounds of the formula: or pharmaceutically acceptable salts thereof, wherein m, n, X, Y, Z, Ar, R1, R2, R3, R4, R5, R6 and R7 are defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds.Type: GrantFiled: August 17, 2007Date of Patent: July 13, 2010Assignee: Roche Palo Alto LLCInventors: David Scott Carter, Ryan Craig Schoenfeld, Robert James Weikert
-
Publication number: 20100168105Abstract: Disclosed herein is at least one piperidine derivative, at least one pharmaceutical composition comprising at least one piperidine derivative disclosed herein for treating at least one histamine H3 receptor associated condition therewithType: ApplicationFiled: May 23, 2008Publication date: July 1, 2010Inventors: Peter Bernstein, Dean Brown, Joseph Cacciola, Phil Edwards, James Folmer, Thierry Groblewski, Mark Sylvester, Steven Wesolowski
-
Publication number: 20100160337Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein Y, R1, R2, R3, R4, RA, and RB are defined herein.Type: ApplicationFiled: December 15, 2009Publication date: June 24, 2010Inventor: Jay M. Matthews
-
Patent number: 7741321Abstract: Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.Type: GrantFiled: November 8, 2006Date of Patent: June 22, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Sara S. Hadida Ruah, Matthew Hamilton, Mark Miller, Peter D. J. Grootenhuis, Brian Bear, Jason McCartney, Jinglan Zhou
-
Publication number: 20100119503Abstract: The present invention is directed to compounds of Formula I: which are modulators of chemokine receptors. The compounds of the invention, and compositions thereof, are useful in the treatment of diseases related to chemokine receptor expression and/or activity.Type: ApplicationFiled: September 25, 2008Publication date: May 13, 2010Applicant: INCYTE CORPORATIONInventors: Chu-Biao Xue, Changsheng Zheng, Hao Feng, Michael Xia, Joseph Glenn, Ganfeng Cao, Brian W. Metcalf
-
Patent number: 7713978Abstract: The present invention relates to compounds of formula (I) processes for their preparation, pharmaceutical compositions containing the same and to their use in the treatment of gastrointestinal and other disorders.Type: GrantFiled: March 29, 2007Date of Patent: May 11, 2010Inventors: Nigel Paul King, Jason Witherington
-
Publication number: 20100093753Abstract: The invention provides compounds of formula I: wherein a, b, c, m, n, q, r, W, Z1, Ar1, Z2, Y, R1, R2, and R3 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.Type: ApplicationFiled: December 17, 2009Publication date: April 15, 2010Applicant: THERAVANCE, INC.Inventors: YongQi Mu, Yu-Hua Ji, Mathai Mammen, Viengkham Malathong
-
Publication number: 20100087435Abstract: Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.Type: ApplicationFiled: December 4, 2009Publication date: April 8, 2010Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Sara Hadida Ruah, Matthew Hamilton, Mark Miller, Peter D.J. Grootenhuis, Brian Bear, Jason McCartney, Jinglan Zhou, Fredrick van Goor
-
Publication number: 20100056541Abstract: The invention provides compounds of formula I: wherein a, b, c, m, n, q, r, W, Z1, Ar1, Z2, R1, R2, and R3 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.Type: ApplicationFiled: October 26, 2009Publication date: March 4, 2010Applicant: THERAVANCE, INC.Inventors: YongQi Mu, Yu-Hua Ji, Mathai Mammen, Viengkham Malathong
-
Patent number: 7671056Abstract: The present invention relates to novel piperazine-piperidine compounds. The compounds are useful as 5-HT1A binding agents, particularly as 5-HT1A receptor antagonists and agonists. These compounds are useful in treating central nervous system disorders, such as cognition disorders, anxiety disorders, depression and sexual dysfunction. The invention relates to compounds and pharmaceutically acceptable salts of formula (I?): wherein R1-R16, Ra, Rb, and n are set forth in the specification. The invention also relates to pharmaceutical compositions comprising compounds and pharmaceutically acceptable salts of formula (I?).Type: GrantFiled: June 9, 2006Date of Patent: March 2, 2010Assignee: Wyeth LLCInventors: Magda Asselin, George Theodore Grosu, Annmarie Louise Sabb, Wayne Everett Childers, Lisa Marie Havran, Zhongqi Shen, James Jacob Bicksler, Dan Chaekoo Chong
-
Publication number: 20100041642Abstract: Urea containing compounds that inhibit MAP kinases, pharmaceutical compositions including such compounds and methods for using these compounds to treat inflammatory diseases and cancer are described herein.Type: ApplicationFiled: August 15, 2009Publication date: February 18, 2010Applicant: LOCUS PHARMACEUTICALS, INC.Inventors: Duyan NGUYEN, Martha KELLY, Kristofer MOFFETT, Enrique Luis MICHELOTTI, Bin Liu
-
Publication number: 20100035849Abstract: The present invention provides novel methylenedioxy phenolic compounds and their derivatives, methods of making them and methods of using them to treat or prevent cardiovascular disease, vascular disease and/or inflammatory disease, as well as Type I and Type II Diabetes and Dyslipidemia patients at risk for hypertension, stroke, cardiovascular and renal disease.Type: ApplicationFiled: August 5, 2009Publication date: February 11, 2010Applicants: OHIO STATE UNIVERSITY RESEARCH FOUNDATION, INVASC THERAPEUTICS, INC.Inventors: Sampath Parthasarathy, Sanjay Rajagopalan, Desikan Rajagopal
-
Patent number: 7659268Abstract: Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.Type: GrantFiled: May 18, 2007Date of Patent: February 9, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Sara Hadida-Ruah, Matthew Hamilton, Mark Miller, Peter D. J. Grootenhuis, Brian Bear, Jason McCartney, Jinglan Zhou, Frederick van Goor
-
Publication number: 20100009972Abstract: A novel pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate compound and its pharmaceutically acceptable salt has a potent FAAH-inhibitory activity. Further, the pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate compound of the present disclosure is also useful in the treatment of urinary frequency and urinary incontinence, overactive bladder and/or pain.Type: ApplicationFiled: August 19, 2009Publication date: January 14, 2010Inventors: Takahiro Ishii, Takashi Sugane, Jun Maeda, Fumie Narazaki, Akio Kakefuda, Kentaro Sato, Tatsuhisa Takahashi, Takatoshi Kanayama, Chikashi Saitoh, Jotaro Suzuki, Chisato Kanai
-
Publication number: 20090306079Abstract: There are disclosed compounds of the formula or a pharmaceutically acceptable salt or solvate thereof which are useful for the treatment of chemokine-mediated diseases such as acute and chronic inflammatory disorders and cancer.Type: ApplicationFiled: January 13, 2009Publication date: December 10, 2009Inventors: Arthur G. Taveras, Cynthia J. Aki, Richard W. Bond, Jianping Chao, Michael Dwyer, Johan A. Ferreira, Jianhua Chao, Younong Yu, John J. Baldwin, Bernd Kaiser, Ge Li, J. Robert Merritt, Purakkattle J. Biju, Kingsley H. Nelson, JR., Laura L. Rokosz, Gaifa Lai, James P. Jakway, Minglang Wu, Evan A. Hecker, Daniel Lundell, Jay S. Fine
-
Patent number: 7629341Abstract: The present invention provides compounds useful for inhibiting the ADAM-10 protein, with selectivity versus MMP-1. Such compounds are useful in the in vitro study of the role of ADAM-10 (and its inhibition) in biological processes. The present invention also comprises pharmaceutical compositions comprising one or more ADAM-10 inhibitors according to the invention in combination with a pharmaceutically acceptable carrier. Such compositions are useful for the treatment of cancer, arthritis, and diseases related to angiogenesis. Correspondingly, the invention also comprises methods of treating forms of cancer, arthritis, and diseases related to angiogenesis in which ADAM-10 plays a critical role.Type: GrantFiled: June 11, 2003Date of Patent: December 8, 2009Assignee: Symphony Evolution, Inc.Inventors: Lynne Canne Bannen, Erick W. Co, Vasu Jammalamadaka, John M. Nuss, Moon Hwan Kim, Donna Tra Le, Amy Lew, Shumeye Mamo, Zhaoyang Wen, Wei Xu
-
Publication number: 20090281086Abstract: A compound of the formula (I): and pharmaceutically acceptable salts thereof, wherein: HetA is a C5 arylene group, wherein the two substituent groups are on adjacent ring atoms, and where the group is further optionally substituted by one halo, amino or C1-7 alkoxy group; Y is —CRC1RC2—(CH2)m—, where m is 0 or 1, RC1 is selected from H, CH3 and CF3, and RC2 is selected from H and CH3, or RC1 and RC2 together with the carbon atom to which they are attached form the 1,1-cyclopropylene group formula (A): RN1 and RN2 are independently selected from H and R, where R is optionally substituted C1-10 alkyl, C3-20 heterocyclyl and C5-20 aryl; or RN1 and RN2, together with the nitrogen atom to which they are attached form an optionally substituted 5-7 membered, nitrogen containing, heterocylic ring; HetB is selected from: (i), where Y1 and Y3 are independently selected from CH and N, Y2 is selected from CX and N and X is H, Cl or F; and (ii), (aa), (bb) Q is O or S.Type: ApplicationFiled: June 15, 2007Publication date: November 12, 2009Applicant: KUDOS PHARMACEUTICALS LIMITEDInventors: Muhammad Hashim Javaid, Xiao-Ling Fan Cockcroft, Keith Allan Menear, Niall Morrison Barr Martin
-
Publication number: 20090281087Abstract: 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: November 12, 2009Applicant: Biovitrum ABInventors: Joseph W. Boyd, Giles A. Brown, Michael Higginbottom, Viet-Anh Anne Horgan (nee Nguyen), Jaqueline Ouzman, Iain Simpson
-
Publication number: 20090270366Abstract: Benzoimidazole compounds, compositions, and methods of using them in leukocyte recruitment inhibition, in modulating H4 receptor, and in treating conditions such as inflammation, H4 receptor-mediated conditions, and related conditions.Type: ApplicationFiled: August 26, 2008Publication date: October 29, 2009Inventors: James P. Edwards, Michael D. Hack, David E. Kindrachuk, Jennifer D. Venable
-
Publication number: 20090264404Abstract: A heterocyclic compound or a salt thereof represented by the formula (1): where R2 represents a hydrogen atom or a lower alkyl group; A represents a lower alkylene group or lower alkenylene group; and R1 represents an aromatic group or a heterocyclic group. The compound of the present invention has a wide treatment spectrum for mental disorders including central nervous system disorders, no side effects and high safety.Type: ApplicationFiled: August 31, 2006Publication date: October 22, 2009Inventors: Hiroshi Yamashita, Hideaki Kuroda, Nobuaki Ito, Shin Miyamura, Kunio Oshima, Jun Matsubara, Haruka Takahashi, Tae Fukushima, Satoshi Shimizu, Kazumi Kondo, Yohji Sakurai, Takeshi Kuroda, Shinichi Taira, Motohiro Itotani, Tatsuyoshi Tanaka
-
Publication number: 20090246137Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: ApplicationFiled: March 25, 2009Publication date: October 1, 2009Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Sara Hadida Ruah, Mark Miller, Jinglan Zhou, Brian Bear, Peter Grootenhuis
-
Publication number: 20090247544Abstract: Certain substituted urea derivatives modulate diskeletal myosin, skeletal actin, skeletal tropomyosin, skeletal troponin C, skeletal troponin I, skeletal troponin T, and skeletal muscle, including fragments and isoforms thereof, as well as the skeletal sarcomere, and are useful in the treatment of obesity, sarcopenia, wasting syndrome, frailty, muscle spasm, cachexia, neuromuscular diseases (e.g., amyotrophic lateral sclerosis, spinal muscular atrophy, familial or acquired myopathies or muscular dystrophies), post-surgical and post-traumatic muscle weakness, and other conditions.Type: ApplicationFiled: February 13, 2009Publication date: October 1, 2009Inventors: Bradley P. MORGAN, Fady MALIK, David J. MORGANS, JR.
-
Selected CGRP antagonists, processes for preparing them and their use as pharmaceutical compositions
Patent number: 7595312Abstract: The present invention relates to CGRP antagonists of general formula wherein A, U, V, W, X and R1 to R3 are defined as in claim 1, the tautomers, diastereomers, enantiomers, hydrates, mixtures thereof and the salts thereof as well as the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids, pharmaceutical compositions containing these compounds, the use thereof and processes for preparing them.Type: GrantFiled: October 16, 2003Date of Patent: September 29, 2009Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Klaus Rudolf, Stephan Georg Mueller, Dirk Stenkamp, Philipp Lustenberger, Alexander Dreyer, Eckhart Bauer, Marcus Schindler, Kirsten Arndt, Henri Doods -
Patent number: 7592347Abstract: The present invention relates to novel piperidine carbonyl piperazine derivatives having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of neurological and psychiatric disorders.Type: GrantFiled: April 21, 2004Date of Patent: September 22, 2009Assignee: Glaxo Group LimitedInventors: Gordon Bruton, Barry Sidney Orlek, Kishore Kalidas Rana
-
Publication number: 20090215794Abstract: Novel piperazine derivatives are provided having the formula wherein R1 is cyano, nitro, trifluoromethyl or halogen, or pharmaceutically acceptable acid addition salts thereof, which are useful as 5-HT1A receptor antagonists.Type: ApplicationFiled: May 5, 2009Publication date: August 27, 2009Applicant: WyethInventors: Wayne E. Childers, Michael G. Kelly, Sharon J. Rosenzweig-Lipson
-
Publication number: 20090203676Abstract: Compounds of formula (I): or pharmaceutically acceptable salts thereof, are GPCR agonists and are useful as for the treatment of obesity and diabetes.Type: ApplicationFiled: June 30, 2006Publication date: August 13, 2009Inventors: Oscar Barba, Stuart Edward Bradley, Matthew Colin Thor Fyfe, Lisa Sarah Bertram, William Gattrell, Martin James Procter, Chrystelle Marie Rasamison, Simon Andrew Swain
-
Patent number: 7572786Abstract: This invention concerns substituted 1-piperidin-3-yl-4-piperidin-4-yl-piperazine derivatives having neurokinin antagonistic activity, in particular NK1 antagonistic activity, a combined NK1/NK3 antagonistic activity and a combined NK1/NK2/NK3 antagonistic activity, their preparation, compositions comprising them and their use as a medicine, in particular for the treatment of schizophrenia, emesis, anxiety and depression, irritable bowel syndrom (IBS), circadian rhythm disturbances, visceral pain, neurogenic inflammation, asthma, micturition disorders such as urinary incontinence and nociception. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in claim 1.Type: GrantFiled: December 17, 2003Date of Patent: August 11, 2009Assignee: Janssen Pharmaceutica, N.V.Inventors: Frans Eduard Janssens, Francois Maria Sommen, Benoît Christian Albert Ghislain De Boeck, Joseph Elisabeth Leenaerts
-
Novel 3-Bicyclocarbonylaminopyridine-2-Carboxamides or 3-Bicyclocarbonylaminopyrazine-2-Carboxamides
Publication number: 20090181968Abstract: The present invention relates to compounds of formula (I) [Chemical formula should be inserted here. Please see paper copy] as well as pharmaceutically acceptable salts and pharmaceutical compositions including the compounds are prepared or thereof: wherein, A1, A2, R1, R2, R3, R4, and R5 and n are as defined in the specification. The compounds of formula (I) are useful in therapy.Type: ApplicationFiled: November 22, 2006Publication date: July 16, 2009Applicant: ASTRAZENECA ABInventors: Kosrat Amin, Johan Broddefalk, Yantao Chen, Karolina Nilsson, Claire Milburn, Helene Desfosses, Ziping Liu, Maxime Tremblay, Christopher Walpole, Zhong-yong Wei, Hua Yang -
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
-
Publication number: 20090176768Abstract: Diaza heterocyclic amide derivatives according to Formula (I) have therapeutic utility, particularly in the treatment of diabetes, obesity and related conditions and disorders: where R5, R6, R7, R8, R9, R10, m, Q, X, and Y are set forth in the description.Type: ApplicationFiled: March 17, 2009Publication date: July 9, 2009Inventors: JAY P. POWERS, Daqing Sun, Xuelei Yan
-
Publication number: 20090176761Abstract: This invention relates to a method of treating and/or preventing endometriosis comprising administering a JNK inhibitor. The JNK inhibitor can also be administered combined with a hormonal suppressor.Type: ApplicationFiled: July 12, 2006Publication date: July 9, 2009Applicant: LABORATORIES SERONO SAInventors: Stephen S. Palmer, Selvaraj Nataraja
-
Publication number: 20090170850Abstract: The present invention provides an cycloalkyl derivative of 3-hydroxy-4-pyridinone which is useful for the chelation of metal ions such as iron. Its preparation and use is described. In particular, the invention concerns the removal of iron in chemical and biological systems including chelating agents having the formula I wherein R1 is X with the proviso that R2 is Y; or R1 is T with the proviso that R2 is W; or R1 is X with the proviso that R2R5N when taken together form a heterocyclic ring selected from piperidinyl, morpholinyl, pyrrolidinyl or piperazinyl, wherein the group piperidinyl, morpholinyl, pyrrolidinyl or piperazinyl is either unsubstituted or substituted with one to three C1 to C6 alkyl groups.Type: ApplicationFiled: May 9, 2008Publication date: July 2, 2009Inventors: Tim Fat Tam, Michael Spino, Wanren Li, Yingsheng Wang, Yanqing Zhao, Birenkumar Hasmukhbhai Shah
-
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
-
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
-
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
-
Publication number: 20090099199Abstract: The invention relates to compound of the formula I wherein the substituents are as defined in the specification; 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: October 15, 2008Publication date: April 16, 2009Inventors: Joachim Nozulak, David Orain, Simona Cotesta
-
Publication number: 20090082362Abstract: Disclosed are diaryl piperazines and related compounds. These compounds are selective modulators of capsaicin receptors, including human capsaicin receptors, that are, therefore, useful in the treatment of a chronic and acute pain conditions, itch and urinary incontinence. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds of the invention are also useful as probes for the localization of capsaicin receptors and as standards in assays for capsaicin receptor binding and capsaicin receptor mediated cation conductance. Methods of using the compounds in receptor localization studies are given.Type: ApplicationFiled: March 28, 2008Publication date: March 26, 2009Inventors: Rajagopal Bakthavatchalam, Alan Hutchison, Robert W. DeSimone, Kevin J. Hodgetts, James E. Krause, Geoffrey G. White
-
Patent number: 7485644Abstract: The invention provides compounds of formula (I): or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein ring B represents a monocyclic aryl ring having six ring atoms or a monocyclic heteroaryl ring having up to six ring atoms and containing one or more ring heteroatoms wherein each said heteroatom is nitrogen; R2 represents a group selected from C1-6 alkyl or aryl, which said group is substituted by one or more fluorine groups; n is 1, 2 or 3; and R1 represents an optionally substituted group selected from C1-6 alkyl, C5-7 cycloalkyl, heterocycloalkyl, aryl, heteroaryl, C1-6 alkyl-aryl, C1-6 alkyl-heteroaryl, C1-6 alkyl-cycloalkyl or C1-6 alkyl-heterocycloalkyl. Processes for their preparation; pharmaceutical compositions containing them; and their use in the treatment of a disease condition mediated by one or more metalloproteinase enzymes.Type: GrantFiled: June 23, 2004Date of Patent: February 3, 2009Assignee: AstraZeneca ABInventors: Maurice Raymond Verschoyle Finlay, David Waterson
-
Publication number: 20090029971Abstract: Compounds as modulators of peroxisome proliferator activated receptors, pharmaceutical compositions comprising the same, and methods of treating disease using the same are disclosed.Type: ApplicationFiled: September 4, 2008Publication date: January 29, 2009Applicant: KALYPSYS, INC.Inventors: Stewart A. Noble, Guy Oshiro, James W. Malecha, Cunxiang Zhao, Carmen Robinson, Sergio G. Duron, Michael Sertic, Andrew K. Lindstrom, Andrew K. Shiau, Christopher D. Bayne, Mehmet Kahraman, Boliang Lou, Steve P. Govek
-
Publication number: 20090029979Abstract: This invention relates to compounds which bind to serotonin receptors inside or outside the central nervous system, in particular compounds which bind to the 5-HT2 or 5-HT7 receptors, their preparation and use, compositions containing them, and methods of treatment using them.Type: ApplicationFiled: July 7, 2006Publication date: January 29, 2009Applicant: BIO-MEDISINSK INNOVASJON ASInventors: Jo Klaveness, Bjarne Brudeli, Finn Olav Levy