1,3,4-oxadiazoles (including Hydrogenated) Patents (Class 548/143)
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Patent number: 7956060Abstract: The present invention provides an antitumor agent and the like, which comprises as an active ingredient, a pyrimidine derivative represented by Formula (I): [wherein —X—Y—Z— represents —O—CR3?N— (wherein R3 represents a hydrogen atom, a substituted or unsubstituted aromatic heterocyclic group and the like) and the like, R1 represents —NR10R11 (wherein R10 and R11 may be the same or different, and each represents a hydrogen atom, substituted or unsubstituted lower alkyl and the like) and the like, R2 represents —NR13R14 (wherein R13 and R14 may be the same or different, and each represents a hydrogen atom, substituted or unsubstituted lower alkyl and the like)] or a pharmaceutically acceptable salt thereof.Type: GrantFiled: March 30, 2005Date of Patent: June 7, 2011Assignee: Kyowa Hakko Kirin Co., Ltd.Inventors: Hitoshi Arai, Tsutomu Matsumura, Syoichi Isami, Hiroshi Ishida, Koji Hagihara, Hiroshi Umehara, Yoshinori Yamashita, Nana Oiwa, Yukimasa Shiotsu, Tomoki Naoe, Hitoshi Kiyoi
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Publication number: 20110124622Abstract: The invention relates to isoindolones of formula, (I) with anti-cancer and/or anti-inflammatory activity and more specifically with MEK kinase inhibitory activity. The invention provides compositions and methods useful for inhibiting abnormal cell growth, treating a hyperproliferative disorder, or treating an inflammatory disease in a mammal. The invention also relates to methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.Type: ApplicationFiled: July 1, 2009Publication date: May 26, 2011Applicant: Genentech, Inc.Inventors: Emanuela Gancia, Robert Andrew Heald, Philip Jackson, Stephen Price
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Patent number: 7943645Abstract: This invention relates to N-aroyl cyclic amine derivatives and their use as pharmaceuticals, specifically as orexin receptor antagonists.Type: GrantFiled: July 8, 2008Date of Patent: May 17, 2011Assignee: SmithKline Beecham LimitedInventors: Wai Ngor Chan, Amanda Johns, Christopher Norbert Johnson, Riccardo Novelli, Roderick Alan Porter
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Publication number: 20110105460Abstract: [Problem] A compound, which can be used for preventing or treating diseases, in which 11?-hydroxysteroid dehydrogenase type 1 (11?-HSD1) is concerned, in particular, diabetes, insulin resistance, dementia, schizophrenia and depression, is provided. [Means for Solution] It was found that a triazole derivative, in which one of the 3- and 5-positions of the triazole ring has (di)alkylmethyl or cycloalkyl, each of which is substituted with —O— (aryl or a heterocyclic group, each of which may be substituted, or lower alkylene-cycloalkyl), and the other thereof has aryl, a heterocyclic group or cycloalkyl, each of which may be substituted, or a pharmaceutically acceptable salt thereof exhibits potent 11?-HSD1 inhibitory action. From the above, the triazole derivative of the present invention can be used for preventing or treating diabetes, insulin resistance, dementia, schizophrenia and depression.Type: ApplicationFiled: July 2, 2009Publication date: May 5, 2011Applicant: ASTELLAS PHARMA INC.Inventors: Seiji Yoshimura, Noriyuki Kawano, Tomoaki Kawano, Daisuke Sasuga, Takanori Koike, Hideyuki Watanabe, Hiroki Fukudome, Nobuyuki Shiraishi, Ryosuke Munakata, Hiroaki Hoshii, Kayoko Mihara
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Publication number: 20110101312Abstract: This invention relates to deuterated indolocarbazole compounds that are useful in electronic applications. It also relates to electronic devices in which the active layer includes such a deuterated compound.Type: ApplicationFiled: December 21, 2009Publication date: May 5, 2011Applicant: E. I. DU PONT DE NEMOURS AND COMPANYInventors: Daniel David LeCloux, Kalindi Dogra, Weishi Wu, Adam Fenninmore, Eric Maurice Smith
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Patent number: 7928140Abstract: The present invention comprises a new class of compounds capable of modulating the activity of PI3 kinase and, accordingly, useful for treatment of PI3 kinase mediated diseases, including melanomas, carcinomas and other cancer-related conditions. The compounds have a general Formula I wherein each of A1, A2, A3, A4, X, R1 and R2 are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of PI3 kinase mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.Type: GrantFiled: August 1, 2008Date of Patent: April 19, 2011Assignee: Amgen Inc.Inventors: Shon Booker, Noel D'Angelo, Derin C. D'Amico, Tae-Seong Kim, Longbin Liu, Kristin Meagher, Mark H. Norman, Kathleen Panter, Laurie B. Schenkel, Adrian L. Smith, Nuria A. Tamayo, Douglas A. Whittington, Ning Xi, Kevin Yang
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Publication number: 20110076291Abstract: Benzoxepin compounds of Formula I, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, wherein: Z1 is CR1 or N; Z2 is CR2 or N; Z3 is CR3 or N; Z4 is CR4 or N; and where (i) X1 is N and X2 is S, (ii) X1 is S and X2 is N, (iii) X1 is CR7 and X2 is S, (iv) X1 is S and X2 is CR7; (v) X1 is NR8 and X2 is N, (vi) X1 is N and X2 is NR8, (vii) X1 is CR7 and X2 is O, (viii) X1 is O and X2 is CR7, (ix) X1 is CR7 and X2 is C(R7)2, (x) X1 is C(R7)2 and X2 is CR7; (xi) X1 is N and X2 is O, or (xii) X1 is O and X2 is N, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: ApplicationFiled: September 27, 2010Publication date: March 31, 2011Inventors: Nicole Blaquiere, Steven Do, Danette Dudley, Adrian Folkes, Richard Goldsmith, Robert Heald, Timothy Heffron, Aleksandr Kolesnikov, Chudi Ndubaku, Alan G. Olivero, Stephen Price, Steven Staben, BinQing Wei
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Publication number: 20110077409Abstract: Cyano-substituted sulfilimines are produced efficiently and in high yield from the corresponding sulfides by reaction with cyanamide and hypochlorite.Type: ApplicationFiled: November 18, 2010Publication date: March 31, 2011Inventors: David E. Podhorez, Ronald Ross, JR., James R. McConnell
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Publication number: 20110077251Abstract: The invention relates to 17? lupane derivatives of formula (I): wherein R1 and X are as defined herein, and pharmaceutically acceptable salts and solvates thereof. These compounds exhibit significant anti-HIV activity. Thus, the invention also relates to methods for prevention or treatment of HIV infection by administering therapeutically effective amounts of a compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof to a subject in need of such treatment.Type: ApplicationFiled: August 16, 2010Publication date: March 31, 2011Inventors: Christophe Moinet, Bingcan Liu, Liliane Halab, Nathalie Turcotte, Real Denis, Carl Poisson, Paul Nguyen-Ba, Monica Bubenik, Laval Chan Chun Kong
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Patent number: 7915298Abstract: This invention provides novel salt and crystalline forms thereof of (?)4-(4-fluorophenyl)-7-[({5-[1-hydroxy-1-(trifluoromethyl)propyl]-1,3,4-oxadiazol-2-yl}amino)-methyl]-2H-chromen-2-one. The compounds are 5-LO inhibitors and are useful for treatment of conditions such as asthma, allergic rhinitis, COPD, and atherosclerosis.Type: GrantFiled: September 24, 2008Date of Patent: March 29, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Francis Gosselin, Vicky Vydra
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Patent number: 7915402Abstract: This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.Type: GrantFiled: April 20, 2009Date of Patent: March 29, 2011Assignee: Reata Pharmaceuticals, Inc.Inventors: Eric Anderson, Xin Jiang, Xiaofeng Liu, Melean Visnick
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Publication number: 20110071196Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.Type: ApplicationFiled: September 15, 2010Publication date: March 24, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Alessandra BARTOLOZZI, Doris RIETHER, Renee M. ZINDELL, Patricia AMOUZEGH, Nigel James BLUMIRE, Monika ERMANN, Innocent MUSHI, Robert John SCOTT
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Patent number: 7906546Abstract: The present invention relates to compounds of the formula (I) wherein R1, R2, R3, R4, R5, X1, X2, X3, X4, n, and k are defined in the description and claims, and pharmaceutically acceptable salts and/or pharmaceutically acceptable esters thereof. The compounds are useful for in the treatment and prophylaxis of diseases which are modulated by LXR? and/or LXR? agonists, including increased lipid and cholesterol levels, particularly low HDL-cholesterol, high LDL-cholesterol, atherosclerotic diseases, diabetes, particularly non-insulin dependent diabetes mellitus, metabolic syndrome, dyslipidemia, Alzheimer's disease, sepsis, inflammatory diseases such as colitis, pancreatitis, cholestasis/fibrosis of the liver, and diseases that have an inflammatory component such as Alzheimer's disease or impaired/improvable cognitive function.Type: GrantFiled: May 6, 2010Date of Patent: March 15, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Henrietta Dehmlow, Bernd Kuhn, Raffaello Masciadri, Narendra Panday, Hasane Ratni, Matthew Blake Wright
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Publication number: 20110053943Abstract: This invention relates to novel compounds of the invention pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.Type: ApplicationFiled: June 1, 2010Publication date: March 3, 2011Inventors: David A. Claremon, Colin M. Tice, Linghang Zhuang, Katerina Leftheris, Yuanjie Ye, Suresh B. Singh
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Publication number: 20110053936Abstract: The present disclosure is directed to new inhibitors of the p38 mitogen-activated protein kinase having the general formula (I), processes for preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: April 3, 2009Publication date: March 3, 2011Inventors: Paul Robert Eastwood, Jacob Gonzalez Rodriguez, Bernat Vidal Juan, Nuria Aguilar Izquierdo
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Publication number: 20110039874Abstract: Disclosed are compounds and compositions that inhibit the action of monoacylglycerol lipase (MGL) and fatty acid amide hydrolase (FAAH), methods of inhibiting MGL and FAAH, methods of modulating cannabinoid receptors, and methods of treating various disorders related to the modulation of cannabinoid receptors.Type: ApplicationFiled: April 16, 2010Publication date: February 17, 2011Applicant: Northeastern UniversityInventors: Alexandros Makriyannis, Spyridon P. Nikas, Shakiru O. Alapafuja, Vidyanand G. Shukla
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Publication number: 20110028447Abstract: This invention relates to compounds, pharmaceutical compositions and methods for the treatment of a condition mediated by CB1 receptor activity in a mammalian subject including a human, which comprises administering to a mammal in need of such treatment a therapeutically effective amount of the compound of formula (I) wherein R1, R2 and R3 are as defined in this specification.Type: ApplicationFiled: February 26, 2009Publication date: February 3, 2011Inventors: Ingrid Price Buchler, Michael Joseph Hayes, Shridhar Gajanan Hegde, Susan Landis Hockerman, Darin Eugene Jones, Steven Wade Kortum, Joseph Gerace Rico, Ruth Elizabeth TenBrink, Kun Ken Wu
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Patent number: 7879850Abstract: The present invention provides compounds of the following structure; A-Q-B—C-D that are useful for treating conditions or disorders associated with DGAT1 activity in animals, particularly humans.Type: GrantFiled: September 26, 2008Date of Patent: February 1, 2011Assignee: Novartis AGInventors: Young-Shin Kwak, Gary Mark Coppola
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Publication number: 20100331335Abstract: The present disclosure provides inhibitors of c-Jun N-terminal kinases (JNK) having a structure according to the following formula: or a salt or solvate thereof, wherein ring A, Ca, Cb, Z, R5, W and Cy are defined herein. The disclosure further provides pharmaceutical compositions including the compounds of the present disclosure and methods of making and using the compounds and compositions of the present disclosure, e.g., in the treatment and prevention of various disorders, such as Alzheimer's disease.Type: ApplicationFiled: February 5, 2010Publication date: December 30, 2010Inventors: Hing L. Sham, Roy K. Hom, Andrei W. Konradi, Gary D. Probst, Simeon Bowers, Anh Truong, R. Jeffrey Neitz, Jennifer Sealy, Gergely Toth
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Patent number: 7855220Abstract: Bicyclic derivatives useful as ion channel antagonists are disclosed herein. The compositions thereof are useful for treating or relieving pain-related conditions.Type: GrantFiled: September 8, 2006Date of Patent: December 21, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Timothy Neubert, Nicole Zimmermann, Esther Martinborough, Aarti Kawatkar, Andreas Termin
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Patent number: 7847100Abstract: The present invention is directed to 1,3,5-phenyl substituted derivative compounds which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.Type: GrantFiled: April 15, 2005Date of Patent: December 7, 2010Assignee: Merck, Sharp & Dohme, Inc.Inventors: James C. Barrow, Georgia B. McGaughey, Philippe G. Nantermet, Hemaka A. Rajapakse, Harold G. Selnick, Shaun R. Stauffer, Craig A. Coburn
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Patent number: 7846956Abstract: The present invention provides a malononitrile compound represented by the formula (I): wherein any one of X1, X2, X3 and X4 is CR100, wherein R100 is a group represented by the formula: the other three of X1, X2, X3 and X4 each represent nitrogen or CR5, provided that 1 to 3 of X1, X2, X3 and X4 represent nitrogen, and Z represents oxygen, sulfur or NR6, which has pest-controlling activity.Type: GrantFiled: January 13, 2005Date of Patent: December 7, 2010Assignee: Sumitomo Chemical Company, LimitedInventors: Hiromasa Mitsudera, Ken Otaka, Jun Fujiwara
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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: 20100292274Abstract: A new class of haloalkyl heteroaryl benzamides is described. These compounds show strong activity against hepatitis viruses.Type: ApplicationFiled: May 11, 2010Publication date: November 18, 2010Inventors: Jean-Francois Rossignol, J. Edward Semple
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Publication number: 20100292187Abstract: 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: June 14, 2010Publication date: November 18, 2010Applicant: PTC THERAPEUTICS, INC.Inventors: Gary M. Karp, Peter Seongwoo Hwang, James J. Takasugi, Hongyu Ren, Richard Gerald Wilde, Anthony A. Turpoff, Alexander Arefolov, Guangming Chen, Jeffrey A. Campbell, Chunshi Li, Steven Paget, Nanjing Zhang, Xiaoyan Zhang, Jin Zhu
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Publication number: 20100286211Abstract: The present invention relates to certain substituted phenyl oxazolidinones and to processes for the synthesis of the same. This invention also relates to pharmaceutical compositions containing the compounds of the present invention as antimicrobials. The compounds are useful antimicrobial agents, effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria, for example, multiple-resistant staphylococci, streptococci and enterococci as well as anaerobic organisms, for example, Bacterioides spp. and Clostridia spp. species, and acid fast organisms, for example, Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp.Type: ApplicationFiled: October 6, 2005Publication date: November 11, 2010Inventors: Biswajit Das, Shahadal Ahmed, Ajay Singh Yadav, Soma Ghosh, Arti Gujrati, Pankaj Sharma, Ashok Rattan
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Publication number: 20100280000Abstract: Disclosed herein are compounds of formula I in which R1, R2, R3, R4, R5, A, X, Y are as described in the specification, their use in pharmaceutical compositions and in methods of treatment or prophylaxis of a melanin-concentrating hormone related disease or condition.Type: ApplicationFiled: April 30, 2010Publication date: November 4, 2010Applicant: AstraZeneca ABInventors: Lars Anders Mikael JOHANSSON, Robert Andrew Judkins, Lanna Li, Bjorn Christian Ingvar Lofberg, Joachim Persson
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Patent number: 7820663Abstract: The present invention is related substituted enaminones represented by a compound of Formula I that are novel allosteric modulators of ?7 nAChRs. The invention also discloses the treatment of disorders that are responsive to enhancement of acetylcholine action on ?7 nAChRs in a mammal by administering an effective amount of a compound of Formula I.Type: GrantFiled: June 15, 2006Date of Patent: October 26, 2010Assignee: The Regents of the University of CaliforniaInventors: Derk J. Hogenkamp, Timothy B. C. Johnstone, Kelvin W. Gee
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Publication number: 20100267710Abstract: Disclosed are compounds of the Formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein W, R1, R2, R7, R8, R9 and R10 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals. Also disclosed is a method of using such compounds in the treatment of hyperproliferative diseases in mammals, and pharmaceutical compositions containing such compounds.Type: ApplicationFiled: June 28, 2010Publication date: October 21, 2010Applicant: ARRAY BIOPHARMA INC.Inventors: Eli M. Wallace, Joseph P. Lyssikatos, Allison L. Marlow, T. Brian Hurley
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Publication number: 20100261717Abstract: Disclosed are compounds of the Formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein W, R1, R2, R7, R8, R9 and R10 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals. Also disclosed is a method of using such compounds in the treatment of hyperproliferative diseases in mammals, and pharmaceutical compositions containing such compounds.Type: ApplicationFiled: June 28, 2010Publication date: October 14, 2010Applicant: ARRAY BIOPHARMA INC.Inventors: Eli M. Wallace, Joseph P. Lyssikatos, Allison L. Marlow, T. Brian Hurley
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Patent number: 7812341Abstract: The present invention relates to a compound having an oxadiazole ring structure having a substituted pyridyl group connected thereto, represented by the following general formula (1). According to the present invention, it becomes possible to provide an organic compound having excellent characteristic of high stability in a thin film state, and the emission efficiency and durability of conventional organic EL devices can be remarkably improved.Type: GrantFiled: March 25, 2005Date of Patent: October 12, 2010Assignee: Hodogaya Chemical Co., Ltd.Inventors: Tetsuzo Miki, Makoto Nagaoka, Shuichi Hayashi, Yoshio Taniguchi, Musubu Ichikawa
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Publication number: 20100237339Abstract: Disclosed is a carbazole derivative and a light-emitting element, a light-emitting device, and an electronic device using thereof. The carbazole derivative possesses an oxadiazole moiety or a quinoxaline moiety as a heteroaromatic ring having an electron-transporting property and a carbazole moiety having a hole-transporting property. The ability of the carbazole derivative to transport both electrons and holes and its large excitation energy larger than a triplet excitation energy of a phosphorescent compound allow the formation of a phosphorescent light-emitting element having well-controlled carrier balance, which contributes to the formation of light-emitting devices and electronic devices that are capable of being driven at a low voltage, have a long lifetime, and consume low power. The detailed structure of the carbazole derivative is defined in the specification.Type: ApplicationFiled: March 17, 2010Publication date: September 23, 2010Inventors: Hiroko Nomura, Sachiko Kawakami, Nobuharu Ohsawa, Satoshi Seo
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Publication number: 20100240717Abstract: The invention relates to thiophene derivatives of formula (I)/their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunosuppressive agents wherein: A represents *—CO—CH?CH—, *—CO—CH2CH2—, *—CO—CH2—NH—, wherein the sterisks indicate the bond that is linked to the thiophene group of Formula (I), and R1-R3 are as defined in the claims.Type: ApplicationFiled: January 10, 2007Publication date: September 23, 2010Applicant: ACTELION PHARMACEUTICALS LTD.Inventors: Martin Boli, David Lehmann, Boris Mathys, Claus Mueller, Oliver Nayler, Beat Steiner, Jörg Velker
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Publication number: 20100240617Abstract: Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at S1P receptors.Type: ApplicationFiled: February 15, 2010Publication date: September 23, 2010Inventors: Kevin R. Lynch, Timothy L. MacDonald, Kevin Guckian, Edward Yin-shiang Lin, Bin Ma
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Publication number: 20100240659Abstract: Disclosed is a compound which is useful as an 11?-hydroxysteroid dehydrogenase type 1 inhibitor. A compound represented by the formula: , its pharmaceutically acceptable salt, or a solvate thereof, wherein Ring A is a group represented by the formula: Ring B is optionally substituted heteroaryl, provided that optionally substituted isoxazole is excluded, or optionally substituted heterocycle, R1 is hydrogen or optionally substituted alkyl, R2 is —OR5, —SR5, halogen, halogenated alkyl or the like, R3 is optionally substituted alkyl or the like, R4 is optionally substituted alkyl or the like, R5 is optionally substituted alkyl or the like, R6 is hydrogen or the like, R7 and R8 are each independently hydrogen or the like, R10 and R11 are each independently hydrogen or the like, R12 is optionally substituted alkyl or the like, m and p are each independently integer of 1 to 3.Type: ApplicationFiled: May 7, 2008Publication date: September 23, 2010Applicant: SHIONOGI & CO., LTD.Inventors: Koji Masuda, Tomoyuki Ogawa, Takuji Nakatani
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Patent number: 7799820Abstract: Disclosed is a compound represented by the formula (I) below, which has a glucokinase-activating effect and is thus useful for treatment of diabetes or obesity, or a pharmaceutically acceptable salt thereof. In the formula, R1 represents an aryl or the like; R11 represents an aryl or the like; R2 represents a formyl or the like, R3 represents a C1-6 alkyl or the like; R3 represents a hydrogen atom or the like; Z1 represents —O— or the like; Z2 represents —O— or the like; Y1-Y4 respectively represent a carbon atom or a nitrogen atom; ring A represents a heteroaryl group; X represents a carbon atom or the like; m represents an integer of 0-2; and q represents an integer of 0-2.Type: GrantFiled: September 29, 2006Date of Patent: September 21, 2010Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Keiji Takahashi, Yoshio Ogino, Teruyuki Nishimura
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Publication number: 20100234417Abstract: A hetero-dimeric or hetero-oligomeric receptor, comprising at least one thyrotropin releasing hormone receptor subunit associated with at least one orexin receptor subunit.Type: ApplicationFiled: November 9, 2007Publication date: September 16, 2010Applicant: DIMERIX BIOSCIENCE PTY LTD.Inventors: Kevin Donald George Pfleger, Ruth Marie Seeber, Heng See Boon, Karin Ann Eidne
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Publication number: 20100234404Abstract: Compounds and compositions for modulating the activity of p38 kinases are provided, including p38?, and p38? kinase. Methods for treating, preventing or ameliorating one or more symptoms of a p38 kinase mediated disease or disorder are also provided.Type: ApplicationFiled: May 28, 2010Publication date: September 16, 2010Inventors: Hengyuan Lang, Jiong Lan, Yungeng Fang
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Publication number: 20100233116Abstract: The present invention provides heterocyclic derivatives hat modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also encompassed.Type: ApplicationFiled: August 13, 2007Publication date: September 16, 2010Inventors: Natalie Dales, Julia Fonarev, Jianmin Fu, Rajender Kamboj, Vishnumurthy Kodumuru, Shifeng Liu, Natalia Pokrovskaia, Vandna Raina, Shaoyi Sun, Zaihui Zhang
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Patent number: 7795283Abstract: Compounds of formula (I), and salts and pro-drugs thereof: Formula (I) wherein for example R1 is optionally substituted aryl or heteroaryl; Y is a linking group selected from, for example, a direct bond, and a (substituted) alkyl chain; R2 is an optionally substituted aryl, an optionally substituted cycloalkyl or an optionally substituted heterocyclic group; are described. Processes to make such compounds and their use as DGAT inhibitors, for example in the treatment of obesity, are also described.Type: GrantFiled: December 9, 2005Date of Patent: September 14, 2010Assignee: AstraZeneca ABInventors: Alan Martin Birch, Suzanne Saxon Bowker, Roger John Butlin, Craig Samuel Donald, William McCoull, Thorsten Nowak, Alleyn Plowright
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Publication number: 20100222398Abstract: This invention relates to novel 1,2,3-triazole derivatives, which are found to be modulators of the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.Type: ApplicationFiled: August 6, 2008Publication date: September 2, 2010Applicant: NeuroSearch A/SInventors: Antonio Nardi, Jeppe Kejser Christensen, Dan Peters, Gunnar M. Olsen, Tino Dyhring
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Publication number: 20100216833Abstract: The present invention relates to compounds of the formula (I) wherein R1, R2, R3, R4, R5, X1, X2, X3, X4, n, and k are defined in the description and claims, and pharmaceutically acceptable salts and/or pharmaceutically acceptable esters thereof. The compounds are useful for in the treatment and prophylaxis of diseases which are modulated by LXR? and/or LXR? agonists, including increased lipid and cholesterol levels, particularly low HDL-cholesterol, high LDL-cholesterol, atherosclerotic diseases, diabetes, particularly non-insulin dependent diabetes mellitus, metabolic syndrome, dyslipidemia, Alzheimer's disease, sepsis, inflammatory diseases such as colitis, pancreatitis, cholestasis/fibrosis of the liver, and diseases that have an inflammatory component such as Alzheimer's disease or impaired/improvable cognitive function.Type: ApplicationFiled: May 6, 2010Publication date: August 26, 2010Inventors: Henrietta Dehmlow, Bernd Kuhn, Raffaello Masciadri, Narendra Panday, Hasane Ratni, Matthew Blake Wright
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Patent number: 7781460Abstract: The present invention relates to isoxazoline derivatives of structure Ia, which can be used as selective inhibitors of phosphodiesterase (PDE) type IV. Compounds disclosed herein can be useful in the treatment of CNS disorders, AIDS, asthma, arthritis, bronchitis, chronic obstructive pulmonary disease (COPD), psoriasis, allergic rhinitis, shock, atopic dermatitis, Crohn's disease, adult respiratory distress syndrome (ARDS), eosinophilic granuloma, allergic conjunctivitis, osteoarthritis, ulcerative colitis and other inflammatory diseases especially in humans. Processes for the preparation of disclosed compounds are provided, as well as pharmaceutical compositions containing the disclosed compounds, and their use as phosphodiesterase (PDE) type IV inhibitors.Type: GrantFiled: August 30, 2006Date of Patent: August 24, 2010Assignee: Ranbaxy Laboratories LimitedInventors: Venkata Palle, Sarala Balachandran, Lalit Kumar Baregama, Saswati Chakladar, Sarika Ramnani, Nagarajan Muthukamal, Abhijit Ray, Sunanda G. Dastidar
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Publication number: 20100204199Abstract: Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-Beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds have the structure: enantiomers, diastereomers, solvates, or salts thereof, wherein A, W, X and Z are defined herein.Type: ApplicationFiled: April 14, 2010Publication date: August 12, 2010Inventors: Xiang-Yang Ye, Jeffrey A. Robl, Ronald L. Hanson, Zhiwei Guo, Ramesh N. Patel
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Publication number: 20100197749Abstract: The invention relates to chemical compounds of formula (I) and (II): or pharmaceutically acceptable salts thereof, which possess Edg-1 antagonistic activity and are accordingly useful for their anti-cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm-blooded animal such as man.Type: ApplicationFiled: January 15, 2007Publication date: August 5, 2010Applicant: ASTRAZENECA ABInventors: Scott Cowen, Tracey Deegan, Gurmit Grewal, Vibha Oza, Jamal Carlos Saeh, Qibin Su
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Publication number: 20100197655Abstract: The present invention relates to compounds of the formula and pharmaceutically acceptable salts, solvates or tautomers thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds, and the uses of such compounds, in particular for the treatment of pain.Type: ApplicationFiled: January 12, 2010Publication date: August 5, 2010Inventors: Serge Beaudoin, Michael Christopher Laufersweiler, Christopher John Markworth, Brian Edward Marron, David Simon Millan, David James Rawson, Steven Michael Reister, Kosuke Sasaki, Robert Ian Storer, Paul Anthony Stupple, Nigel Alan Swain, Christopher William West, Shulan Zhou
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Patent number: 7763732Abstract: Disclosed herein are indole derivatives of the formula (I) wherein each of the substitutents is given the definition as set forth in the specification and claims. Also disclosed are pharmaceutical compositions containing the indole derivatives and use of the derivatives for the treatment of pain.Type: GrantFiled: August 18, 2006Date of Patent: July 27, 2010Assignee: N.V. OrganonInventors: Paul David Ratcliffe, Julia Adam-Worrall, Angus John Morrison, Stuart John Francis, Takao Kiyoi
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Publication number: 20100184813Abstract: DGAT-1 inhibitor compounds of formula (I) and pharmaceutically-acceptable salts thereof are described, together with pharmaceutical compositions, processes for making them and their use in treating, for example, obesity wherein n is 0, 1, 2 or 3, R is independently selected from fluoro, chloro, bromo, trifluoromethyl, methoxy, difluoromethoxy and trifluoromethoxy and Z is carboxy or a mimic or bioisostere thereof, hydroxyl, hydroxymethyl, or —CONRbRc wherein Rb and Rc are independently selected from hydrogen and (1-4C)alkyl, which (1-4C)alkyl group may be optionally substituted by carboxy or a mimic or bioisostere thereof.Type: ApplicationFiled: December 18, 2009Publication date: July 22, 2010Applicant: AstraZeneca ABInventors: Alan Martin BIRCH, Gary Peter Tomkinson, Sharmistha Pal, Anna Pettersen
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Patent number: 7759377Abstract: Compounds of formula (I) as defined herein: inhibit the formation of the ?-amyloid peptide (?-A4) and are, therefore, useful in the treatment of pathologies in which a ?-amyloid peptide (?-A4) formation inhibitor provides a therapeutic benefit. Particular such pathologies are senile dementia, Alzheimer's disease, Down's syndrome, Parkinson's disease, amyloid angiopathy, cerebrovascular disorders, frontotemporal dementias and Pick's disease, post-traumatic dementias, pathologies linked to neuroinflammatory processes, Huntington's disease and Korsakov's syndrome.Type: GrantFiled: March 20, 2008Date of Patent: July 20, 2010Assignee: Sanofi-AventisInventors: Sylvie Baltzer, Marc Pascal, Viviane Van Dorsselaer
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Publication number: 20100168189Abstract: Therapeutic compounds, compositions, methods, and medicaments related thereto are disclosed herein.Type: ApplicationFiled: February 8, 2008Publication date: July 1, 2010Inventors: David W. Old, Wha Bin Im, Vinh X. Ngo