Chalcogen Attached Indirectly To The Diazole Ring By Acyclic Nonionic Bonding Patents (Class 548/310.1)
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Patent number: 8410283Abstract: An electrolyte additive is selected from N-alkyl benzimidazole derivatives and is applicable to dye-sensitized solar cells. Accordingly, the electrolyte additive can be added to electrolyte at low concentration, and loss of function due to crystallization after long-term use can be prevented; in addition, short circuit photocurrent density and solar energy-to-electricity conversion efficiency of solar cells incorporating the electrolyte additive can be increased.Type: GrantFiled: July 15, 2010Date of Patent: April 2, 2013Assignee: National Taipei University of TechnologyInventors: Sheng-Tung Huang, Chung-Kuang Yang
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Publication number: 20130065896Abstract: Provided is a novel compound which shows an antagonistic effect against T-type calcium channels, and is useful as a pharmaceutical product. A compound represented by general formula (I), and a pharmaceutical agent containing the same, are disclosed: wherein n represents the number of nitrogen atoms contained in the 6-membered fused aromatic ring, and is 0, 1 or 2; p represents the number of nitrogen atoms contained in the 6-membered aromatic ring, and is 0 or 1; X represents an oxygen atom, —SO2— or —N(R9)—; and R1 to R5 each represents a hydrogen atom or other substituents.Type: ApplicationFiled: May 24, 2011Publication date: March 14, 2013Applicant: TOA Eiyo Ltd.Inventors: Hidekazu Masaki, Hiroshi Takasugi, Tomoyuki Nagayama, Ryutaro Shimono, Yujiro Uchino, Koichi Takayanagi
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Publication number: 20130056075Abstract: Provided is a compound of formula (I): wherein A is C2-3 alkylene; m is an integer ranging from 2 to 25; and n is an integer ranging from 3 to 10. An electrolyte for a dye-sensitized solar cell having the compound of formula (I) and/or a compound of formula (II) is further provided for increasing photoelectric conversion efficiency.Type: ApplicationFiled: September 4, 2012Publication date: March 7, 2013Applicant: EVERLIGHT USA, INC.Inventors: Yu-Hui Lee, Hsin-Ying Lu, Kuan-Wei Lee, Tzu-Heng Ko
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Publication number: 20130035337Abstract: The present invention relates to a novel fused bicyclic heteroaryl derivative or a pharmacologically acceptable salt thereof, which has an excellent hypoglycemic effect or treats and/or prevents the onset of a disorder of carbohydrate or lipid metabolism or a disease mediated by peroxisome proliferator-activated receptor (PPAR) ?. A compound having the general formula (I): wherein R1 represents a C1-C6 alkyl group, a C6-C10 aryl group which may be substituted with 1 to 5 group(s) independently selected from Substituent Group a, or the like; R2 represents a C1-C6 alkyl group; R3 represents a C6-C10 aryl group which may be substituted with 1 to 5 group(s) independently selected from Substituent Group a, or the like; Q represents a group represented by the formula ?CH— or a nitrogen atom; and Substituent Group a represents a halogen atom, a C1-C6 alkyl group, a C1-C6 hydroxyalkyl group, and the like, or a pharmacologically acceptable salt thereof.Type: ApplicationFiled: March 13, 2012Publication date: February 7, 2013Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Kousei Shimada, Yoshiyuki Onishi, Makoto Mori, Eri Tokumaru
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Publication number: 20130029964Abstract: An object of the present invention is to provide a novel low molecular weight compound exhibiting an osteogenesis-promoting action. This object is achieved by a compound having the general formula (I) or a pharmacologically acceptable salt thereof. In the general formula (I), R1 and R2 represent hydrogen atoms, and the like; R3 represents a hydrogen atom, and the like; X, Y, and Z represent nitrogen atoms, and the like; A represents a phenylene group, and the like; n represents 1 or 2, and the like; and V and W represent oxygen atoms, and the like.Type: ApplicationFiled: August 27, 2012Publication date: January 31, 2013Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Kazumasa Aoki, Satoshi Matsui, Kenji Yoshikawa, Hiroki Shimizu, Junko Sasaki, Katsuyoshi Nakajima, Osamu Kanno, Kiyoshi Oizumi
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Patent number: 8242157Abstract: 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 R0, R1, R2, R3, R4 and a are defined herein.Type: GrantFiled: June 10, 2010Date of Patent: August 14, 2012Assignee: Janssen Pharmaceutica NVInventors: Michele C. Jetter, Mark J. Macielag, Mingde Xia, Xiaoqing Xu
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Publication number: 20120165543Abstract: Methods are provided for the production of bendamustine alkyl ester, bendamustine, as well as derivatives thereof. With the methods the production of these compounds is possible in reproducibly high yields. To this end, hydroxyl-group-containing esters are used as the starting material, whose hydroxyl groups are substituted in a simple way by halogen groups. This substitution is possible in the presence of (i) oxalyl chloride and (ii) dialkylformamide, dialkyl acetamide or dimethyl sulfoxide. In a subsequent reaction, the resulting esters can be hydrolyzed to form the acid.Type: ApplicationFiled: December 22, 2011Publication date: June 28, 2012Applicant: HERAEUS PRECIOUS METALS GMBH & CO. KGInventors: Kai GROH, Holger RAUTER, Dirk BORN
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Publication number: 20120071532Abstract: Novel solid forms of bendamustine hydrochloride are described, as well as methods of their preparation and use.Type: ApplicationFiled: November 22, 2011Publication date: March 22, 2012Applicant: CEPHALON, INC.Inventors: Martin Ian Cooper, Laurent D. Courvoisier, Mark Eddleston, Robert E. McKean
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Publication number: 20120046307Abstract: The invention provides specific small molecule compounds that allosterically regulate the activity or modulate protein-protein interactions of AGC protein kinases and the Aurora family of protein kinases, methods for their production, pharmaceutical compositions comprising same, and their use for preparing medicaments for the treatment and prevention of diseases related to abnormal activities of AGC protein kinases or of protein kinases of the Aurora family.Type: ApplicationFiled: October 16, 2009Publication date: February 23, 2012Applicant: UNIVERSITAET DES SAARLANDESInventors: Matthias Engel, Wolfgang Fröhner, Adriane Stroba, Ricardo M. Biondi
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Publication number: 20120029026Abstract: The present invention relates to a novel pyridine derivative or a pharmacologically acceptable ester thereof, or a pharmacologically acceptable salt of the derivative or ester, which has an excellent hypoglycemic effect or treats and/or prevents the onset of a disorder of carbohydrate or lipid metabolism or a disease mediated by peroxisome proliferator-activated receptor (PPAR) ?. A compound represented by the general formula (I): [wherein R represents a pyridyl group substituted with 1 to 3 group(s) independently selected from Substituent Group A, and Substituent Group A represents a halogen atom, a C1-C6 alkyl group and a C1-C6 alkoxy group] or a pharmacologically acceptable ester thereof, or a pharmacologically acceptable salt of the compound or ester.Type: ApplicationFiled: April 15, 2011Publication date: February 2, 2012Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Tsuyoshi SHINOZUKA, Tomoharu TSUKADA, Kunihiko FUJII, Makoto MORI
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Publication number: 20110318807Abstract: Ghrelin O-acyltransferase (GOAT) is inhibited with designed small molecules. Methods comprise contacting the GOAT with an inhibitor and detecting a resultant inhibition.Type: ApplicationFiled: September 6, 2011Publication date: December 29, 2011Inventors: Patrick G. Harran, Michael S. Brown, Joseph L. Goldstein, Jin Yang, Tong-Jin Zhao
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Publication number: 20110282066Abstract: [Object] A screening method for a compound which is useful as an agent for treating 17?HSD type 5-related diseases and/or an agent for treating 17?HSD type 5-related cancer such as prostate cancer is provided. [Means for Solution] The present invention has been completed by establishing a screening method for a compound which is useful for treating 17?HSD type 5-related diseases, by manifesting a tumor by transplanting tumor cells to, for example, an immunodeficient mouse, topically administering a steroid which is a biosynthetic substance for a hormone into the tumor, and measuring the level of a hormone produced in the tumor.Type: ApplicationFiled: January 26, 2010Publication date: November 17, 2011Inventors: Takashi Furutani, Kentaro Enjo, Aya Kikuchi, Sadao Kuromitsu, Yukitaka Ideyama, Tomoyuki Suzuki, Ryoko Kurihara
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Patent number: 8030497Abstract: A compound of formula (I) or a pharmaceutically acceptable salt or prodrug ester thereof: wherein R1-R7 are as disclosed in the specification.Type: GrantFiled: January 13, 2005Date of Patent: October 4, 2011Assignee: Novartis AGInventors: Marc Gerspacher, Sven Weiler
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Publication number: 20110230523Abstract: Substituted benzoimidazole compounds useful as anti-infectives that decrease resistance, virulence, or growth of microbes are provided. Methods of making and using substituted benzoimidazole compounds, as well as pharmaceutical preparations thereof, in, e.g., reducing antibiotic resistance and inhibiting biofilms.Type: ApplicationFiled: August 6, 2009Publication date: September 22, 2011Applicant: Paratek Pharmaceuticals, Inc.Inventors: Stuart B. LEVY, Michael N. ALEKSHUN, Brent L. PODLOGAR, Kwasi OHEMENG, Atul K. VERMA, Tadeusz WARCHOL, Beena BHATIA, Todd BOWSER, Mark GRIER
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Patent number: 8003806Abstract: The invention relates to compounds of the Formula 1 and to pharmaceutically acceptable salts and solvates thereof, wherein A, X2, X4, X5 and X1 are as defined herein. The invention also relates to methods of treating abnormal cell growth in mammals by administering the compounds of Formula 1 and to pharmaceutical compositions for treating such disorders which contain the compounds of Formula 1.Type: GrantFiled: November 9, 2005Date of Patent: August 23, 2011Assignee: OSI Pharmaceuticals, LLCInventors: Jason Bloxham, Gary V. Borzillo, Eric William Collington, Shazia Sadiq, Colin Peter Sambrook Smith, Chris L. Waller, Graham M. Wynne
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Publication number: 20110190509Abstract: New methods for the preparation of bendamustine, and the pharmaceutical salts thereof, are described. Novel compounds useful for the preparation of bendamustine are also described.Type: ApplicationFiled: April 5, 2011Publication date: August 4, 2011Applicant: Cephalon, Inc.Inventors: Jian Chen, Katrin Przyuski, Renee Caroline Roemmele
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Patent number: 7981925Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.Type: GrantFiled: August 26, 2009Date of Patent: July 19, 2011Assignee: CalciMedica, Inc.Inventors: Gonul Velicelebi, Kenneth A. Stauderman, Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
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Publication number: 20110166102Abstract: The present invention is directed to a novel 2-substituted benzimidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.Type: ApplicationFiled: March 17, 2011Publication date: July 7, 2011Inventors: Vernon C. ALFORD, JR., James C. LANTER, Raymond A. NG
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Patent number: 7960562Abstract: It is intended to provide a compound useful as a GnRH receptor antagonist. The inventors further investigated propane-1,3-dione derivatives. As a result, they confirmed that a compound having a benzene ring or a thiophene ring substituted with a group represented by —SO2—R3 in a propane-1,3-dione derivative having 2-(1,3-dihydro-2H-benzimidazol-2-ylidene) has an excellent GnRH receptor antagonistic effect and accomplished the present invention. Because the compound of the present invention has a potent GnRH receptor antagonistic effect, it is useful for the treatment of sex hormone-dependent diseases, particularly GnRH-related diseases. Further, because the compound of the present invention has an excellent metabolic stability in human and few drug interactions, therefore it has preferable characteristics as a pharmaceutical used for the above-mentioned diseases.Type: GrantFiled: March 30, 2006Date of Patent: June 14, 2011Assignee: Astellas Pharma Inc.Inventors: Masaaki Hirano, Isao Kinoyama, Shunichiro Matsumoto, Eiji Kawaminami, Kei Ohnuki, Hirofumi Yamamoto, Kazuhiko Osoda, Tatsuhisa Takahashi, Takashi Shin, Takanori Koike, Itsuro Shimada, Hiroyuki Hisamichi, Toshiyuki Kusayama
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Publication number: 20110118219Abstract: Prodrugs of steroidal C-17 benzoazoles, pyrimidinoazoles(azabenzoazoles) and diazines. Methods of synthesis are also described, whereby a prodrug group is substituted for a functional group at A ring portion of the ABC ring structure of the steroid. Suitable prodrug groups include amino acid groups, succinate groups, phosphate groups, or sulfamate groups. The prodrugs of the disclosed compounds allow for improved oral bioavailability of the compounds that are inhibitors of human CYP17 enzyme as well as potent antagonists of both wild type and mutant androgen receptors (AR). The compounds and the corresponding prodrugs are useful for the treatment of conditions such as human prostate cancer, breast cancer, and prostate hyperplasia.Type: ApplicationFiled: March 19, 2009Publication date: May 19, 2011Applicant: UNIVERSITY OF MARYLAND, BALTIMOREInventors: Vincent C.O. Njar, Angela M.H. Brodie, Lalji K. Gediya
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Patent number: 7943781Abstract: A process comprising cyclizing 3-amino-4-butyramido-5-methylbenzoic acid to form 2-n-propyl-4-methyl-benzimidazole-6-carboxylic acid.Type: GrantFiled: October 18, 2005Date of Patent: May 17, 2011Assignees: Dr. Reddy's Laboratories Limited, Dr. Reddy's Laboratories, Inc.Inventors: Sundaram Venkataraman, Vijayavitthal Thippannachar Mathad, Srirami Reddy Kikkuru, Srinivasan Neti, Raveendra Reddy Chinta, Muthulingam Arunagiri, Lalitha Kumari Routhu
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Patent number: 7939672Abstract: Disclosed herein are a new phenylacetate derivative represented by Chemical Formula 1 or pharmaceutically acceptable salt thereof, a preparation method thereof, and a composition for prevention or treatment of diseases induced by the activation of T-type calcium ion channels containing the same. The composition containing the phenylacetate derivative according to the present invention effectively inhibits the activation of T-type calcium ion channels and may be useful in the prevention or treatment of diseases such as hypertension, cancer, epilepsy, and neurogenic pains induced by the activation of T-type calcium ion channels. wherein, X, R1, and R3 are as defined herein.Type: GrantFiled: April 23, 2009Date of Patent: May 10, 2011Assignee: Korea Institute of Science and TechnologyInventors: Kye Jung Shin, Hyung Kook Lee, Eun Joo Roh, Dong Jin Kim, Kyung Il Choi, Hyewhon Rhim, Hye Jin Chung, Seon Hee Seo
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Publication number: 20110105573Abstract: The invention relates to benzimidazole acetic acid compounds which function as antagonists of the Chemoattractant Receptor-homologous molecule expressed on T-Helper type 2 cells (CRTH2) receptor. The invention also relates to the use of these compounds to inhibit the binding of prostaglandin D2 and its metabolites or certain thromboxane metabolites to the CRTH2 receptor and to treat disorders responsive to such inhibition.Type: ApplicationFiled: June 8, 2010Publication date: May 5, 2011Inventors: Youssef L. Bennani, Lawrence Nathan Tumey, Elizabeth Ann Gleason, Michael Joseph Robarge
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Patent number: 7932399Abstract: The present invention is directed to a novel 2-substituted benzimidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.Type: GrantFiled: January 23, 2007Date of Patent: April 26, 2011Assignee: Janssen Pharmaceutica NVInventors: Vernon C. Alford, Jr., James C. Lanter, Raymond A. Ng, Zhihua Sui
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Publication number: 20110065728Abstract: The present invention provides pharmaceutical compositions containing benzene compound(s) represented by General Formula (1) below and, particularly, LPL-activating compositions for use in hyperlipidemia therapeutic and preventive agents, anti-obesity agents, and the like: wherein R1, R2, R3 and R4 are as defined in the specification.Type: ApplicationFiled: May 14, 2008Publication date: March 17, 2011Applicant: OTSUKA PHARMACEUTICAL FACTORY, INC.Inventors: Irina Neagu, Michael Ohlmeyer, Vidyadhar M. Paradkar, Kurt W. Saionz, Koushi Iwata, Takashi Okamura, Tadao Shibutani
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Publication number: 20110034526Abstract: This invention relates generally to benzimidazole-based modulators of Liver X receptors (LXRs) having formula (I) and related methods: wherein R2 is C6-C10 aryl or heteroaryl including 5-10 atoms, each of which is: (i) substituted with 1 R7, and (ii) optionally substituted with from 1-5 Re; and R1, R3, R4, R5, R6, R7, and Re are defined herein.Type: ApplicationFiled: December 19, 2008Publication date: February 10, 2011Applicant: Wyeth LLCInventors: Ronald Charles Bernotas, Jeremy Mark Travins, Jay Edward Wrobel, David Harry Kaufman
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Patent number: 7879895Abstract: The present invention is directed to novel benzimidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.Type: GrantFiled: June 22, 2009Date of Patent: February 1, 2011Assignee: Janssen Pharmaceutica NVInventors: Raymond Ng, Zhihua Sui, Jihua Guan, James C. Lanter, Vernon C. Alford, Jr.
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Publication number: 20110009622Abstract: [Problem] To provide compounds useful as preventives or remedies for circular system disorders, nervous system disorders, metabolic disorders, reproduction system disorders, digestive system disorders, neoplasm, infectious diseases, etc., or as herbicides. [Means for Solution] A long-chain fatty acyl elongase inhibitor comprising, as the active ingredient thereof, a compound or a pharmaceutically-active salt thereof of a formula (I): [wherein W represents a hydrogen atom, a C1-6 alkyl, etc.; X represents an aryl, a heteroaryl, etc.; n indicates 0 or 1; Z represents a hydrogen atom, a C1-6 alkyl, etc.; A1, A2, A3 and A4 each independently represent CH or N].Type: ApplicationFiled: April 17, 2009Publication date: January 13, 2011Inventors: Makoto Jitsuoka, Tsuyoshi Nagase, Nagaaki Sato, Daisuke Tsukahara
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Publication number: 20110003800Abstract: 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 R0, R1, R2, R3, R4 and a are defined herein.Type: ApplicationFiled: June 10, 2010Publication date: January 6, 2011Inventors: Mark J. Macielag, Mingde Xia, Xiaoqing Xu
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Publication number: 20110003801Abstract: 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 R0, R1, R2, R3, R4 and a are defined herein.Type: ApplicationFiled: June 10, 2010Publication date: January 6, 2011Inventors: Michele C. Jetter, Mark J. Macielag, Mingde Xia, Xiaoqing Xu
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Publication number: 20100292276Abstract: The present invention is directed to benzimidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by TRP M8 (transient receptor potential M8 channel). More particularly, the compounds of the present invention are useful in the treatment of inflammatory pain, inflammatory hyperalgesia, inflammatory hypersensitivity condition, neuropathic pain, neuropathic cold allodynia, inflammatory somatic hyperalgesia, inflammatory visceral hyperalgesia, cardiovascular disease aggravated by cold, anxiety and depression.Type: ApplicationFiled: May 4, 2010Publication date: November 18, 2010Inventors: Raul R. Calvo, Sanath K. Meegalla, Mark R. Player
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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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Publication number: 20100248313Abstract: The present invention relates to new optically active heteroaromatic ?-hydroxy esters useful in the synthesis of epothilone derivatives, to certain compounds used to produce these intermediates, as well as to processes for their production.Type: ApplicationFiled: December 18, 2008Publication date: September 30, 2010Inventors: Johannes Platzek, Ludwig Zorn, Bernd Buchmann, Werner Skuballa, Orlin Petrov
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Publication number: 20100210837Abstract: This disclosure describes the molecular cloning of a pactamycin biosynthetic gene cluster from Streptomyces pactum ATCC 27456, characterization of individual genes in the gene cluster and the proteins encoded thereby as well as uses thereof. The pactamycin gene cluster is located within an 86.35 kilobases genetic locus and includes 53 open reading frames, 26 of which are considered to be the core cluster directly involved in the biosynthesis of pactamycin.Type: ApplicationFiled: April 18, 2008Publication date: August 19, 2010Inventor: Taifo Mahmud
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Patent number: 7776900Abstract: This invention relates to novel benzimidazole derivatives, pharmaceutical compositions containing these compounds, and methods of treatment therewith. The compounds of the invention are useful in the treatment of central nervous system diseases and disorders, which are responsive to modulation of the GABAA receptor complex, and in particular for combating anxiety and related diseases.Type: GrantFiled: April 18, 2006Date of Patent: August 17, 2010Assignee: Neurosearch A/SInventors: Lene Teuber, Janus S. Larsen, Philip K. Ahring, Elsebet Østergaard Nielsen, Naheed Mirza
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Publication number: 20100183531Abstract: The invention concerns preparations, particularly cosmetic or pharmaceutical/dermatological preparations, containing phenylbenzimidazole sulfonic acid (i.e. 2-phenylbenzimidazole-5-sulfonic acid) neutralised with basic amino acids such as arginine, lysine, ornithine and histidine so that the pH of the preparation can be at or below 7.0 without incurring crystallisation of the phenylbenzimidazole sulfonic acid.Type: ApplicationFiled: July 9, 2007Publication date: July 22, 2010Applicant: Symrise GmbH & Co. KGInventors: William Johncock, Jürgen Claus
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Patent number: 7759372Abstract: A compound of the formula (I): wherein Z4, Z5 and Z9 each is independently carbon atom or nitrogen atom; Y is hydroxy, mercapto or amino; RA is a group of the formula: (wherein C ring is nitrogen-containing heteroaryl) has an inhibitory activity against integrase.Type: GrantFiled: August 8, 2006Date of Patent: July 20, 2010Assignee: Shionogi & Co., Ltd.Inventors: Masahiro Fuji, Hidenori Mikamiyama, Hitoshi Murai
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Publication number: 20100158996Abstract: A novel therapeutic agent for hyperlipidemia, which is an ester compound represented by the formula (1?) (wherein R1 and R2 are each hydrogen atom or optionally substituted aryl, etc.; X is —COO— or —CON(R10)—; R3 and R4 are each hydrogen atom, C1-C6 alkyl or C1-C6 alkoxy, etc.; R5, R6 and R7 are each hydrogen atom, C1-C6 alkyl or C1-C6 alkoxy, etc.; R9 and R9 are each independently hydrogen atom, C1-C6 alkyl, —CON(R18) (R19) or —COO(R20), etc.; ring A, ring B and ring C are each independently aryl or heterocycle residue, etc.; Alk1 and Alk2 are each independently alkanediyl, etc.; l and m are each an integer of 0 or 1 to 3) or a prodrug thereof, or a pharmaceutically acceptable salt of either. The therapeutic agent selectively inhibits MTP in the small intestine, thus causes no such side effect as a fatty liver.Type: ApplicationFiled: February 12, 2010Publication date: June 24, 2010Inventors: Atsushi Hagiwara, Yasuhiro Ohe, Naoya Odani, Shizue Watanabe, Taku Ikenogami, Takashi Kawai, Kenya Madono, Toshio Taniguchi
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Patent number: 7732618Abstract: The invention relates to benzimidazole acetic acid compounds which function as antagonists of the Chemoattractant Receptor-homologous molecule expressed on T-Helper type 2 cells (CRTH2) receptor. The invention also relates to the use of these compounds to inhibit the binding of prostaglandin D2 and its metabolites or certain thromboxane metabolites to the CRTH2 receptor and to treat disorders responsive to such inhibition.Type: GrantFiled: September 21, 2005Date of Patent: June 8, 2010Assignee: WyethInventors: Youssef L. Bennani, Lawrence Nathan Tumey, Elizabeth Ann Gleason, Michael Joseph Robarge
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Patent number: 7705031Abstract: The present invention relates to compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein the R1, Z, Y, RA, and W groups of formula I are as defined herein. The invention also provides pharmaceutically acceptable compositions and methods of using the compositions in the treatment of various disorders.Type: GrantFiled: November 1, 2007Date of Patent: April 27, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Dean M. Wilson, Andreas P. Termin, Jesus E. Gonzalez, III, Nicole Zimmermann, Yulian Zhang, Lev T. D. Fanning
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Publication number: 20100086955Abstract: Ghrelin O-acyltransferase (GOAT) is inhibited with designed small molecules. Methods comprise contacting the GOAT with an inhibitor and detecting a resultant inhibition.Type: ApplicationFiled: October 1, 2009Publication date: April 8, 2010Inventors: Patrcik G. Harran, Michael S. Brown, Joseph L. Goldstein, Jing Yang, Tong-Jin Zhao
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Publication number: 20100063101Abstract: The invention is concerned with novel benzimidazole derivatives of formula (I) wherein A, n and R1 to R7 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds can be used as medicaments.Type: ApplicationFiled: September 4, 2009Publication date: March 11, 2010Inventors: Gregory Martin Benson, Konrad Bleicher, Song Feng, Uwe Grether, Bernd Kuhn, Rainer E. Martin, Jean-Marc Plancher, Hans Richter, Sven Taylor
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Publication number: 20100048912Abstract: Described are steroidal C-17 benzoazoles, pyrimidinoazoles (azabenzoazoles) and diazines. Methods for their synthesis are also described, which include methods having a step of nucleophilic vinylic “addition-elimination” substitution reaction of 3?-acetoxy-17-chloro-16-formylandrosta-5,16-diene or analogs thereof and benzoazole or pyrimidinoazole nucleophiles and methods having a palladium catalyzed cross-coupling reaction of 17-iodoandrosta-5,16-dien-3?-ol or analogs thereof with tributylstannyl diazines. The compounds are potent inhibitors of human CYP17 enzyme as well as potent antagonists of both wild type and mutant androgen receptors (AR). The compounds are useful for the treatment of human prostate cancer.Type: ApplicationFiled: October 9, 2009Publication date: February 25, 2010Inventors: Angela Brodie, Vincent Njar
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Publication number: 20100048913Abstract: Described are steroidal C-17 benzoazoles, pyrimidinoazoles (azabenzoazoles) and diazines. Methods for their synthesis are also described, which include methods having a step of nucleophilic vinylic “addition-elimination” substitution reaction of 3?-acetoxy-17-chloro-16-formylandrosta-5,16-diene or analogs thereof and benzoazole or pyrimidinoazole nucleophiles and methods having a palladium catalyzed cross-coupling reaction of 17-iodoandrosta-5,16-dien-3?-ol or analogs thereof with tributylstannyl diazines. The compounds are potent inhibitors of human CYP17 enzyme as well as potent antagonists of both wild type and mutant androgen receptors (AR). The compounds are useful for the treatment of human prostate cancer.Type: ApplicationFiled: October 9, 2009Publication date: February 25, 2010Inventors: Angela Brodie, Vincent Njar
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Publication number: 20100048564Abstract: The present invention relates to a novel fused bicyclic heteroaryl derivative or a pharmacologically acceptable salt thereof, which has an excellent hypoglycemic effect or treats and/or prevents the onset of a disorder of carbohydrate or lipid metabolism or a disease mediated by peroxisome proliferator-activated receptor (PPAR) ?. A compound having the general formula (I): wherein R1 represents a C1-C6 alkyl group, a C6-C10 aryl group which may be substituted with 1 to 5 group(s) independently selected from Substituent Group a, or the like; R2 represents a C1-C6 alkyl group; R3 represents a C6-C10 aryl group which may be substituted with 1 to 5 group(s) independently selected from Substituent Group a, or the like; Q represents a group represented by the formula ?CH— or a nitrogen atom; and Substituent Group a represents a halogen atom, a C1-C6 alkyl group, a C1-C6 hydroxyalkyl group, and the like, or a pharmacologically acceptable salt thereof.Type: ApplicationFiled: October 5, 2009Publication date: February 25, 2010Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Kousei SHIMADA, Yoshiyuki ONISHI, Makoto MORI, Eri TOKUMARU
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Publication number: 20100048914Abstract: Described are steroidal C-17 benzoazoles, pyrimidinoazoles (azabenzoazoles) and diazines. Methods for their synthesis are also described, which include methods having a step of nucleophilic vinylic “addition-elimination” substitution reaction of 3?-acetoxy-17-chloro-16-formylandrosta-5,16-diene or analogs thereof and benzoazole or pyrimidinoazole nucleophiles and methods having a palladium catalyzed cross-coupling reaction of 17-iodoandrosta-5,16-dien-3?-ol or analogs thereof with tributylstannyl diazines. The compounds are potent inhibitors of human CYP 17 enzyme as well as potent antagonists of both wild type and mutant androgen receptors (AR). The compounds are useful for the treatment of human prostate cancer.Type: ApplicationFiled: October 9, 2009Publication date: February 25, 2010Inventors: Angela Brodie, Vincent Njar
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Patent number: 7645771Abstract: The present invention relates to compounds of formula (I) or a pharmaceutically acceptable derivatives thereof, useful in the treatment of prophylazis of CCR5-related diseases and disorders, for example, in the inhibition of HIV replication, the prevention or treatment of HIV infection, and in the treatment of the resulting acquired immune deficiency syndrome (AIDS).Type: GrantFiled: December 12, 2003Date of Patent: January 12, 2010Assignee: SmithKline Beecham Corp.Inventors: Wieslaw Mieczyslaw Kazmierski, Chrisopher Joseph Aquino, Neil Bifulco, Eric Eugene Boros, Brian Andrew Chauder, Pek Yoke Chong, Maosheng Duan, Felix Deanda, Jr., Cecilia Suarez Koble, Ed Williams McLean, Jennifer Poole Peckham, Angilique C Perkins, James Benjamin Thompson, Dana Vanderwall
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Publication number: 20100004271Abstract: The invention provides Compounds of formula (I) or pharmaceutically acceptable esters, amides, solvates or salts thereof, including salts of such esters or amides, and solvates of such esters, amides or salts, wherein R3, R4, G, Y, W and R5 are as defined in the specification. The invention also provides the use of such Compounds in the treatment or Prophylaxis of a condition associated with a disease or disorder associated with thyroid receptor activity.Type: ApplicationFiled: July 4, 2006Publication date: January 7, 2010Applicant: KARO BIO ABInventors: Ana Maria Garcia Collazo, Eva Kristina Koch, Anton Joakim Lofstedt, Aiping Cheng, Thomas Fredrik Hansson, Edouard Zamaratski
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Publication number: 20090318514Abstract: The invention provides the use of compounds of formula (I) or pharmaceutically acceptable esters, amides, solvates or salts thereof, including salts of such esters or amides, and solvates of such esters, amides or salts, for the manufacture of a medicament for the treatment or prophylaxis of a condition that may be treated with a thyroid receptor agonist or partial agonist wherein R1, R2, R3, R4, Y, W and R5 are as defined in the specification. The invention also provides compounds of formula (Ia) or pharmaceutically acceptable esters, amides, solvates or salts thereof, including salts of such esters or amides, and solvates of such esters, amides or salts, formula (Ia) wherein R1, R2, R3, R4, Y, W and R5 are as defined in the specification.Type: ApplicationFiled: May 3, 2007Publication date: December 24, 2009Inventors: Ana Maria Garcia Collazo, Eva Kristina Koch, Anton Joakim Löfstedt, Aiping Cheng, Sandra Gordon, Tomas Fredrik Hansson
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Publication number: 20090312384Abstract: A method of providing a cooling sensation to the skin or mucous membranes of the mouth by applying thereto a quantity of at least one chemical compound sufficient to cause a desirable degree of cooling sensation, the chemical compound comprising a compound of formula I: in which R1, R2 are independently in either the meta- or para-position and independently comprise at least one of hydrogen, halide, C1-C3 alkyl (linear or branched), halide, C1-C3 alkoxy, nitro, nitrile, amide or ester; R3 comprises at least one of C1-C5 alkyl or C1-C5 alkenyl groups (linear or branched), R4 comprises at least one of hydrogen, C1-C3 alkyl (linear or branched), or a halide. The cooling effect provided is in some instances superior to that achievable by any of the known commercial cooling agents.Type: ApplicationFiled: July 16, 2007Publication date: December 17, 2009Inventors: Stefan Michael Furrer, Karen Ann Bell, Christophe C. Galopin, Thomas Scott McCluskey, Jay Patrick Slack