1,3-oxazoles (including Hydrogenated) Patents (Class 514/374)
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Patent number: 8486940Abstract: The invention relates to novel pyrrolidine derivatives of formula (I): wherein R1, R2 and R3 are as defined herein, as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5). QC catalyzes the intramolecular cyclization of N-terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N-terminal glutamate residues into pyroglutamic acid under liberation of water.Type: GrantFiled: September 13, 2010Date of Patent: July 16, 2013Assignee: Probiodrug AGInventors: Ulrich Heiser, Daniel Ramsbeck, Robert Sommer, Antje Meyer, Torsten Hoffmann, Livia Boehme, Hans-Ulrich Demuth
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Publication number: 20130172339Abstract: A compound of formula (I), wherein A is S, O or a double bond, and L is a substituted thiazolyl, phenyl or pyridyl. The compound is useful for the treatment of inflammation and cancer.Type: ApplicationFiled: September 19, 2011Publication date: July 4, 2013Applicant: KANCERA ABInventors: Styrbjorn Bystrom, Charles Hedgecock, Evert Homan, Thomas Lundback, Jessica Martinsson, Meral Sari, Katarina Farnegardh, Mattias Jonsson
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Publication number: 20130165488Abstract: The present invention relates to novel TP receptor antagonists, which optionally cross the blood-brain barrier of a mammal. The invention also provides methods for treating a disorder related to activation of TP receptor utilizing the compounds of the invention.Type: ApplicationFiled: February 28, 2013Publication date: June 27, 2013Applicant: The Trustees of the University of PennsylvaniaInventor: The Trustees of the University of Pennsylvania
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Publication number: 20130165443Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted phenyl or optionally substituted pyridinyl, and R2, R3, R4, R5, R6, R7, R8 and R9 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X3 and/or a P2X2/3 receptor antagonists and methods of making the compounds.Type: ApplicationFiled: August 23, 2012Publication date: June 27, 2013Inventors: Chris Allen Broka, Ronald Charles Hawley
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Patent number: 8470813Abstract: The invention relates to a series of thiazoline and oxazoline derivatives, compositions thereof, and methods of treating conditions and disorders using such compounds.Type: GrantFiled: January 28, 2010Date of Patent: June 25, 2013Assignee: AbbVie Inc.Inventors: Ramin Faghih, Gregory A. Gfesser, Christopher L. Lynch, Murali Gopalakrishnan, Sujatha Gopalakrishnan, John Malysz, Earl J. Gubbins, Rachid El Kouhen, Jinhe Li, Kathy A. Sarris, Melissa J. Michmerhuizen, Ying Wang
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Patent number: 8470776Abstract: The present invention provides conjugates of disorazoles and their derivatives with cell-binding molecules, such as peptides, proteins, hormones, blood proteins and antibodies. The present invention further provides novel disorazole derivatives and processes of manufacturing such conjugates and disorazole derivatives. These compounds can be used as medicaments for the treatment of physiological and/or pathophysiological conditions in mammals, in particular for the treatment of various tumors.Type: GrantFiled: March 19, 2010Date of Patent: June 25, 2013Assignee: Aeterna Zentaris GmbHInventors: Eckhard Guenther, Olaf Schaefer, Michael Teifel, Klaus Paulini
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Publication number: 20130158075Abstract: The present invention relates to heterocyclic compounds of formula 1, in all their stereoisomeric and tautomeric forms; and their pharmaceutically acceptable salts, solvates, polymorphs, prodrugs, carboxylic acid isosteres and N-oxides. The invention also relates to processes for the manufacture of the heterocyclic compounds and to pharmaceutical compositions containing them. The said compounds and their pharmaceutical compositions are useful in the prevention and treatment of diseases or disorders mediated by diacylglycerol acyltransferase (DGAT), particularly DGAT1. The present invention further provides a method of treatment of such diseases or disorders by administering a therapeutically effective amount of said compounds or their pharmaceutical compositions, to a mammal in need thereof.Type: ApplicationFiled: August 31, 2011Publication date: June 20, 2013Applicant: PIRAMAL ENTERPRISES LIMITEDInventors: Rajiv Sharma, Kishorkumar Shivajirao Kadam, Ravindra Dnyandev Jadhav, Shivaji Sadashiv Kandre, Amol Gupte
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Publication number: 20130158018Abstract: Disclosed are Cathepsin-S reversible inhibitor compounds of the formula (I) which are useful in the treatment of autoimmune and other diseases. Also disclosed are pharmaceutical compositions containing the same, and methods of making and using the same.Type: ApplicationFiled: March 2, 2011Publication date: June 20, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Michael J. Burke, Derek Cogan, Donghong Amy Gao, Alexander Heim-Riether, Eugene Richard Hickey, Matthew Russell Netherton, Philip Dean Ramsden, David Charles Thompson, Zhaoming Xiong
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Patent number: 8466149Abstract: In its many embodiments, the present invention relates to a novel class of 6-substituted sulfonyl-1,3,3-trialkyl-6-azabicyclo[3.2.1]octane compounds useful to inhibit 11?-hydroxysteroid dehydrogenase type-I, pharmaceutical compositions containing the compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the expression of 11?-hydroxysteroid dehydrogenase type-I using such compounds or pharmaceutical compositions.Type: GrantFiled: August 12, 2008Date of Patent: June 18, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Craig D. Boyle, Samuel Chackalamannil, Unmesh Shah, Claire M. Lankin
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Publication number: 20130150417Abstract: The present invention provides compounds, that are N-alkyl-2-(1-(5-substituted-2-(3-oxo-3-(trifluoromethylsulfon-amido)propyl)benzyppyrrolidin-2-ypoxazole-4-carboxamide wherein the 5 substituent is selected from the group consisting of halo and alkyloxy radicals. The compound may be represented by the following formula wherein R1 is selected from the group consisting of CO2R7 and CON(R7)SO2R7 wherein R1, R2, R3, R4, and R7 are as defined in the specification. The compounds may be administered to treat DP1, FP, EP1, EP3, TP and/or EP4 receptor mediated diseases or conditions.Type: ApplicationFiled: August 19, 2011Publication date: June 13, 2013Applicant: ALLERGAN, INC.Inventors: Jose L. Martos, William R. Carling, David F. Woodward, Jenny W. Wang, Jussi J. Kangasmetsa
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Publication number: 20130150392Abstract: The compound (I) or a salt thereof has an excellent controlling activity against pests. Then the compound (I) or a salt thereof is useful for an active ingredient of a pesticidal composition.Type: ApplicationFiled: February 8, 2013Publication date: June 13, 2013Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventor: SUMITOMO CHEMICAL COMPANY, LIMITED
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Patent number: 8455525Abstract: This invention provides compounds of formulas I, Ia, Ib, Ic, Id, Ie, and or salts thereof, pharmaceutical compositions comprising a compound of formulas I, Ia, Ib, Ic, Id, Ie, and a pharmaceutically acceptable excipient, methods of modulating the androgen receptor, methods of treating diseases beneficially treated by an androgen receptor modulator (e.g., sarcopenia, prostate cancer, contraception, type 2 diabetes related disorders or diseases, anemia, depression, and renal disease) and processes for making compounds of formulas I, Ia, Ib, Ic, Id, Ie, and intermediates useful in the preparation of same.Type: GrantFiled: August 17, 2010Date of Patent: June 4, 2013Assignee: Radius Health, Inc.Inventor: Chris P. Miller
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Publication number: 20130136794Abstract: Heteroaryl(alkyl)dithiocarbamate compounds represented by general formula (I) or their pharmaceutically acceptable salts, their preparing methods, and their uses for preparing antitumor medicines are disclosed, wherein each said substituent is defined as in the description. The compounds are new tyrosine kinase inhibitors useful as an anti-tumor agents, preferably useful in the preparation of medicines for treating breast cancer, liver cancer, non-small cell lung cancer, gastric cancer, colon cancer, leukaemia or nasal cancer.Type: ApplicationFiled: April 21, 2011Publication date: May 30, 2013Applicant: PEKING UNIVERSITYInventors: Runtao Li, Zemei Ge, Jingrong Cui, Xingyl Sun, Zhongqing Wang, Xu Yan
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Patent number: 8450304Abstract: The present invention comprises compounds of Formula (I). wherein: R1, R2, R3, and R4 are as defined in the specification. The invention also comprises pharmaceutical compositions comprising the compounds of formula (I) and methods of preventing, treating or ameliorating a CCR2 mediated syndrome, disorder or disease, for example, type II diabetes, obesity or asthma, by administering the compounds of formula (I).Type: GrantFiled: December 9, 2009Date of Patent: May 28, 2013Assignee: Janssen Pharmaceutica N.V.Inventors: Xuqing Zhang, Heather Rae Hufnagel, Cuifen Hou, Dana L. Johnson, Zhihua Sui, Barry Fegely, David Breslin
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Publication number: 20130131120Abstract: A therapeutic agent or a prophylactic agent for neuropathic pain provides a synergistically-enhanced analgesic effect at a dose at which a calcium channel ?2? ligand does not produce any side effects as well as which agent does not produce any new side effects on the central nervous system. The therapeutic agent or a prophylactic agent for neuropathic pain includes as effective ingredients a cyclohexane derivative, represented by the following formula, or a pharmaceutically acceptable salt thereof or a prodrug thereof, and a calcium channel ?2? ligand.Type: ApplicationFiled: July 29, 2011Publication date: May 23, 2013Applicant: TORAY INDUSTRIES, INC.Inventors: Naoki Izumimoto, Hidenori Mochizuki
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Patent number: 8445521Abstract: A synergistic antimicrobial composition. The composition contains at least two components. The first component is ortho-phenylphenol or its alkali metal or ammonium salts. The second component is 4,4-dimethyloxazolidine (DMOZ).Type: GrantFiled: September 15, 2010Date of Patent: May 21, 2013Assignee: Dow GLobal Technologies LLCInventor: Bei Yin
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Patent number: 8445527Abstract: The present invention provides a method of treating a HCV infection in a subject in need thereof by administering a compound of Formula I: or pharmaceutically acceptable salts thereof or stereoisomers thereof.Type: GrantFiled: May 22, 2012Date of Patent: May 21, 2013Assignee: Novartis AGInventors: Michael Patane, Prakash Raman, David Thomas Parker, Jiping Fu, Branko Radetich, Mohindra Seepersaud, Aregahegn Yifru, Rui Zheng, Trixi Brandl, Francois Lenoir, Pascal Rigollier, Oliver Simic
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Publication number: 20130123243Abstract: This invention is directed to compounds of formula (I): where r, q, R, R2, R3, R4, R5a, R5b, R5c, R6a, R6b, R6c, R7, R8, and R9 are described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, solvates, clathrates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A4 hydrolase inhibitors and therefore useful in treating inflammatory disorders. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.Type: ApplicationFiled: October 18, 2012Publication date: May 16, 2013Inventor: Celtaxsys, Inc.
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Publication number: 20130116227Abstract: Disclosed is a novel biaryl amide derivative represented by formula (1) and having an affinity for the aldosterone receptor; also disclosed is a pharmaceutically acceptable salt thereof. (In the formula, A is any of the groups represented by formula (a); L is —CONH—, etc.; R1 is a substitutable aminosulfonyl group, etc.; R2 is a hydrogen atom, etc.; R3 is a hydrogen atom, etc.; R4 is a hydrogen atom, a halogen atom, hydroxy group, a substitutable amino group, a substitutable C1-6 alkoxy group, a substitutable 4- to 7-membered cyclic amino group, etc.; R5a, R5b and R5c are each independently hydrogen atoms, etc.; R6 is a halogen atom, a cyano group, etc.; R7 and R8 are each independently a hydrogen atom, etc.; and m is an integer such as 0.Type: ApplicationFiled: July 12, 2011Publication date: May 9, 2013Applicant: DAINIPPON SUMITOMO PHARMA CO., LTD.Inventors: Seiji Katayama, Seiji Hori, Futoshi Hasegawa, Kuniko Suzuki
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Patent number: 8435999Abstract: Compositions and processes for controlling nematodes are described herein, e.g., nematodes that infest plants or animals. The compounds include oxazoles, oxadiazoles and thiadiazoles.Type: GrantFiled: August 13, 2008Date of Patent: May 7, 2013Assignee: Monsanto Technology LLCInventors: Deryck J. Williams, Matt W. Dimmic, William P. Haakenson, Jr., Al Wideman, Barry J. Shortt, Tim Cheeseright, Michael J. Crawford
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Patent number: 8436023Abstract: The present invention comprises compounds of Formula (I). wherein: R1, R2, X, and Z are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).Type: GrantFiled: June 9, 2011Date of Patent: May 7, 2013Assignee: Janssen Pharmaceutica N.V.Inventors: Xuqing Zhang, Zhihua Sui, James C. Lanter
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Publication number: 20130109675Abstract: A series of oxazole and thiazole compounds are shown herein to be small molecule inhibitors of the Wnt pathway that specifically target the activity of the stabilized pool of ?-cat oxazole and thiazole compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, cancer, and others.Type: ApplicationFiled: August 27, 2012Publication date: May 2, 2013Inventors: Ramanuj Dasgupta, Foster Gonsalves
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Publication number: 20130109710Abstract: The spiro compound represented by the following general formula [Ia], its pharmaceutically acceptable salt or a solvate thereofType: ApplicationFiled: September 14, 2012Publication date: May 2, 2013Applicant: JAPAN TOBACCO INC.Inventors: Takashi Shimada, Hiroshi Ueno, Kazuhiro Tsutsumi, Kouichi Aoyagi, Tomoyuki Manabe, Shin-Ya Sasaki, Susumu Katoh
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Publication number: 20130102592Abstract: The invention provides a compound which is an amide of the formula (1), or a salt, solvate, N-oxide or tautomer thereof; wherein: a is 0 or 1; b is 0 or 1: provided that the sum of a and b is 0 or 1; T is O or NH Ar1 is a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S, and being optionally substituted en by one or more substituents R1; Ar2 Js a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S and being optionally substituted by one or more substituents R2; and R1 and R2 are as defined in the claims. The compounds are inhibitors of kinases and in particular FLT3, FLT4 and Aurora kinases.Type: ApplicationFiled: December 5, 2012Publication date: April 25, 2013Applicant: SAREUM LIMITEDInventor: Sareum Limited
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Publication number: 20130096127Abstract: The present invention provides a compound of formula I?; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R5, B1, X and n are defined herein. The invention also relates a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: November 29, 2012Publication date: April 18, 2013Applicant: NOVARTIS AGInventor: NOVARTIS AG
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Publication number: 20130096167Abstract: Methods for preserving technical products such as fuels and lubricants with a microbicidal composition. The composition is made up of at least one formaldehyde donor compound and at least one antioxidant. The antioxidant is either a gallic ester, a phenol derivative, a L-ascorbic acid, including salts and derivatives thereof, a tocopherol or one of its associated derivatives.Type: ApplicationFiled: December 4, 2012Publication date: April 18, 2013Applicant: L' AIR LIQUIDE SANTE (INTERNATIONAL)Inventor: L' AIR LIQUIDE SANTE (INTERNATIONAL)
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Publication number: 20130089613Abstract: Phenyl propanoic acid compounds having activating effect on peroxisome proliferator-activated receptors (PPAR?,?,?) and a preparation method and uses thereof are provided in the present invention. The compounds can be used for treating or preventing diseases associated with peroxisome proliferator-activated receptors (PPAR?,?,?).Type: ApplicationFiled: June 18, 2011Publication date: April 11, 2013Applicant: ZHEJIANG HISUN PHARMACEUTICAL CO., LTD.Inventors: Yaping Wang, Guojun Zheng, Peng Sun, Yi Li, Yingqiu Wu, Bin Liu, Xiaoyu Liu, Hua Bai, Hongyan Li, Xiaohe Zheng
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Patent number: 8415359Abstract: The present invention relates to a compound or a pharmacologically acceptable salt thereof having superior glucokinase activating activity, and is a compound represented by general formula (I), or pharmacologically acceptable salt thereof: [wherein, A represents, for example, an oxygen atom or sulfur atom, R1 represents, for example, a C1-C6 alkyl group, a C1-C6 alkoxy group or a C1-C6 halogenated alkyl group, A and R1 together with the carbon atom bonded thereto form a heterocyclic group that may be substituted with 1 to 3 group(s) independently selected from Substituent Group ?, R2 represents a phenyl group that may be substituted with 1 to 5 group(s) independently selected from Substituent Group ? or a heterocyclic group that may be substituted with 1 to 3 group(s) independently selected from Substituent Group ?, R3 represents a hydroxy group or a C1-C6 alkoxy group, and Substituent Group ? consists of, for example, a halogen atom, a C1-C6 alkyl group, a C1-C6 alkyl group substituted with 1 or 2 hydType: GrantFiled: August 5, 2011Date of Patent: April 9, 2013Assignee: Daiichi Sankyo Company, LimitedInventors: Akihiro Furukawa, Takehiro Fukuzaki, Yukari Onishi, Hideki Kobayashi, Takeshi Honda, Yumi Matsui, Masahiro Konishi, Kenjiro Ueda, Tetsuyoshi Matsufuji
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Publication number: 20130085147Abstract: The present disclosure is generally directed to antiviral compounds, and more specifically directed to compounds which can inhibit the function of the NS5A protein encoded by Hepatitis C virus (HCV), compositions comprising such compounds, and methods for inhibiting the function of the NS5A protein.Type: ApplicationFiled: November 7, 2012Publication date: April 4, 2013Applicant: Bristol-Myers Squibb CompanyInventor: Bristol-Myers Squibb Company
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Patent number: 8410023Abstract: Compositions and processes for controlling nematodes are described herein, e.g., nematodes that infest plants or animals. The compounds include oxazoles, oxadiazoles and thiadiazoles.Type: GrantFiled: October 14, 2010Date of Patent: April 2, 2013Assignee: Monsanto Technology LLCInventors: Urszula Slomczynska, Matt W. Dimmic, William P. Haakenson, Jr., Al Wideman
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Patent number: 8404722Abstract: The present invention relates generally to compounds represented in Formula (I), pharmaceutical compositions comprising them and methods of treating of diseases or disorders such as cancer.Type: GrantFiled: March 13, 2009Date of Patent: March 26, 2013Assignee: Amgen Inc.Inventors: Matthew Brown, Michael G. Johnson
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Patent number: 8404728Abstract: This disclosure relates to materials and methods for inhibiting Botulinum neurotoxin, and more particularly to materials and methods for inhibiting the zinc endopeptidase of Botulinum neurotoxin serotypes A, D and/or E (BoNTA, BoNTD and/or BoNTE).Type: GrantFiled: July 29, 2010Date of Patent: March 26, 2013Assignees: Mayo Foundation for Medical Education and Research, U.S. Army Medical Research and Material CommandInventors: Yuan-Ping Pang, Jewn Giew Park, Shaohua Wang, Anuradha Vummenthala, Rajesh K Mishra, Jon Davis, Charles B. Millard, James J. Schmidt
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Publication number: 20130072529Abstract: The invention relates to a pharmaceutical composition comprising aleglitazar and to the process of manufacture and uses thereof.Type: ApplicationFiled: November 12, 2012Publication date: March 21, 2013Applicant: Hoffmann-La Roche Inc.Inventor: Hoffmann-La Roche Inc.
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Publication number: 20130065897Abstract: The present invention provides novel compounds of the Formula I, pharmaceutical compositions comprising such compounds and methods for using such compounds as agents or drugs for inhibiting perforin activity and for treating a subject at risk of or susceptible to a disease or disorder, or having a disease or disorder associated with undesirable perforin activity.Type: ApplicationFiled: December 22, 2010Publication date: March 14, 2013Applicant: PETER MACCALLUM CANCER INSTITUTEInventors: Julie Ann Spicer, Kristiina Maria Huttunen, Dani Michelle Lyons, Joseph Albert Trapani, Mark John Smyth, William Alexander Denny
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Patent number: 8394841Abstract: The invention provides compounds and pharmaceutical compositions thereof, which are useful for modulating G protein-coupled receptor 120 (GPR120), and methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated GPR120.Type: GrantFiled: January 8, 2008Date of Patent: March 12, 2013Assignee: IRM LLCInventors: Robert Epple, Mihai Azimioara, Christopher Cow, Ross Russo, Victor Nikulin, Gerald Lelais
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Patent number: 8394787Abstract: The invention relates to compounds of the general formula (I) where: R2 is a hydrogen or fluorine atom or a hydroxyl, cyano, trifluoromethyl, C1-6-alkyl, C1-6-alkoxy, or NR8R9 group; m, n, o and p independently are a number from 0 to 3, provided that m+n?7 and that o+p?7; A is a covalent bond, an oxygen atom, a C1-6-alkylene group or a —O—C1-6-alkylene group in which the end that is an oxygen atom is bonded to the R1 group and the end that is an alkylene group is bonded to the carbon of the bicyclic compound; R1 is an optionally substituted aryl or heteroaryl group; R3 is a hydrogen or fluorine atom or a C1-6-alkyl or trifluoromethyl group; R4 is an optionally substituted 5-membered heterocyclic compounds; wherein the compounds can be in the state of a base or an acid addition salt. The invention can be used in therapeutics.Type: GrantFiled: May 11, 2010Date of Patent: March 12, 2013Assignee: SanofiInventors: Ahmed Abouabdellah, Nathalie Chereze, Aude Fayol, Alistair Lochead, Mourad Saady, Julien Vache, Philippe Yaiche
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Publication number: 20130053364Abstract: The invention provides sulphone compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making various sulphone compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2.Type: ApplicationFiled: April 23, 2012Publication date: February 28, 2013Inventors: Hazel J. Dyke, Susan M. Cramp, Thomas D. Pallin, Janusz J. Kulagowski, John G. Montana, Robert Zahler
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Publication number: 20130053386Abstract: The invention encompasses a novel class of diaryl ether derivatives which inhibit the processing of APP by the putative ?-secretase while sparing Notch signaling pathway, and thus are useful in the treatment or prevention of Alzheimer's disease without the development of Notch inhibition mediated gastrointestinal issues. Pharmaceutical compositions and methods of use are also included.Type: ApplicationFiled: October 5, 2010Publication date: February 28, 2013Inventors: William Colby Brown, Richard W. Heidebrecht, Jason Brubaker, Christian Fischer, John T. Hendrix, Elizabeth H. Kelley, Rachel N. MacCoss, Joey L. Methot, Thomas Miller, Karin M. Otte, Phieng Siliphaivanh, Thomas Reger, Peter D. Williams, Catherine M. Wiscount
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Publication number: 20130053416Abstract: 3-Heteroaroylamino-propionic acid derivatives and their use as pharmaceuticals The present invention relates to compounds of the formula I, wherein Ht, G, R10, R30, R40, R50 and R60 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin A, and are useful for the treatment of diseases such as atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.Type: ApplicationFiled: July 26, 2012Publication date: February 28, 2013Applicant: SANOFIInventors: Sven RUF, Josef PERNERSTORFER, Thorsten SADOWSKI, Georg HORSTICK, Herman SCHREUDER, Christian BUNING, Klaus WIRTH
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Publication number: 20130053423Abstract: Cosmetic compositions comprising substituted amino heterocyclic carbamoyl analogs and methods of using such compositions to impart anti-aging benefits to the skin are disclosed. The substituted amino heterocyclic carbamoyl analogs are believed to have modulatory activity against one or more biochemical pathways implicated in skin aging.Type: ApplicationFiled: August 25, 2011Publication date: February 28, 2013Applicant: AVON PRODUCTS, INC.Inventor: John W. Lyga
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Publication number: 20130053387Abstract: Disclosed herein are new compounds of desazadesferrothiocin polyether (DADFT-PE) analogues, as well as pharmaceutical compositions comprising them and their application as metal chelation agents for the treatment of disease. Methods of chelation of iron and other metals in a human or animal subject are also provided for the treatment of metal overload and toxicity.Type: ApplicationFiled: May 4, 2011Publication date: February 28, 2013Applicant: FerroKin BioScience, Inc.Inventor: James W. Malecha
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Publication number: 20130045914Abstract: In its many embodiments, the present invention provides a novel class of biaryl spiroaminooxazoline analogues as modulators of ?2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the ?2C adrenergic receptors using such compounds or pharmaceutical compositions.Type: ApplicationFiled: October 18, 2012Publication date: February 21, 2013Applicant: Merck Sharp & Dohme CorpInventor: Merck Sharp & Dohme Corp.
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Patent number: 8377942Abstract: Novel isoxazoline compounds, compositions containing the compounds and methods for making the compounds are disclosed. The compounds and compositions have pesticidal properties and are suitable for controlling ectoparasites on non-human animals.Type: GrantFiled: December 17, 2009Date of Patent: February 19, 2013Assignee: Novartis AGInventors: Steve Nanchen, Noëlle Gauvry, Francois Pautrat
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Patent number: 8372871Abstract: Compounds of general formula (I) below: are characterized in that A represents in particular a C5-C10 heterocyclic group, Y represents in particular a single bond, and B represents in particular an aryl or heteroaryl group.Type: GrantFiled: November 10, 2009Date of Patent: February 12, 2013Assignee: Centre National de la Recherche ScientifiqueInventors: Jean-Yves Winum, Jean-Louis Montero, Stephan Köhler
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Patent number: 8367708Abstract: The present invention relates to a compound represented by formula (I), which has a GPR120 agonist action and thus is useful for treatment of diabetes mellitus or hyperlipidemia, or a pharmaceutically acceptable salt thereof. In the formula, (AA) represents a phenyl or the like, which may be substituted with a lower alkoxy group or the like; (BB) represents a divalent group or the like, derived by removal of two hydrogen atoms from a benzene which may be substituted with a halogen atom or the like; X represents a spacer having a main chain composed of 1-8 carbon atoms wherein 1-3 carbon atoms in the main chain may be substituted with an oxygen atom or the like; and Y represents a hydrogen atom or the like.Type: GrantFiled: November 29, 2007Date of Patent: February 5, 2013Assignee: MSD K.K.Inventors: Noriaki Hashimoto, Yasuhiro Sasaki, Chisato Nakama, Makoto Ishikawa
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Publication number: 20130029966Abstract: The invention relates to novel oxindole derivatives of general formula (I), wherein the substituents R1, R2, A, B, and Y are defined as in Claim 1. The invention further relates to medicaments containing said derivatives, and use thereof for the prevention and/or treatment of vasopressin-dependent diseases.Type: ApplicationFiled: September 23, 2011Publication date: January 31, 2013Applicant: Abbott GmbH & Co. KGInventors: Thorsten Oost, Wilfried Lubisch, Wilfried Hornberger, Liliane Unger, Herve Geneste, Astrid Netz
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Publication number: 20130030027Abstract: The present invention is directed to hemi phorboxazole A: and its stereoisomers, as well as derivatives of hemi phorboxazole A of formula I: wherein ring A is aryl or a 5- or 6-membered heteroaryl optionally substituted with one or more of halogen, —OH, or —C1-6alkyl; and R is —CN, a 5- or 6-membered heteroaryl, or halogen; and the pharmaceutically acceptable salt forms thereof, in addition to methods of using these compounds.Type: ApplicationFiled: July 23, 2010Publication date: January 31, 2013Applicants: The Regents of the University of California, The Trustes of The University of PennsylvaniaInventors: Amos B. Smith, III, Zhuqing Liu, Anne-Marie L. Hogan, Doralyn S. Dalisay, Tadeusz F. Molinski
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Publication number: 20130030022Abstract: 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 26, 2012Publication date: January 31, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventor: Boehringer Ingelheim International GmbH
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Patent number: 8362020Abstract: The present disclosure is generally directed to antiviral compounds, and more specifically directed to compounds which can inhibit the function of the NS5A protein encoded by Hepatitis C virus (HCV), compositions comprising such compounds, and methods for inhibiting the function of the NS5A protein.Type: GrantFiled: December 21, 2010Date of Patent: January 29, 2013Assignee: Bristol-Myers Squibb CompanyInventors: Omar D. Lopez, Denis R. St. Laurent, Jason Goodrich, Jeffrey Lee Romine, Michael Serrano-Wu, Fukang Yang, Ramesh Kakarla, Xuejie Yang, Yuping Qiu, Lawrence B. Snyder
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Patent number: 8362003Abstract: The present invention relates to 3-aminopyrrolidine derivatives of the formula I: (wherein R1, R2, R3, R4, R5, R6, R7, R8, X, Y and X are as defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of chemokine receptors and more specifically as a modulator of the CCR2 and/or CCR5 receptor. The compounds and compositions of the invention may bind to chemokine receptors, e.g., the CCR2 and/or CCR5 chemokine receptors, and are useful for treating diseases associated with chemokine, e.g., CCR2 and/or CCR5, activity, such as atherosclerosis, restenosis, lupus, organ transplant rejection and rheumatoid arthritis.Type: GrantFiled: June 16, 2011Date of Patent: January 29, 2013Assignee: Incyte CorporationInventors: Chu-Biao Xue, Brian W. Metcalf, Hao Feng, Ganfeng Cao, Taisheng Huang, Changsheng Zheng, Darius J. Robinson, Amy Qi Han