Cyano Or -c(=x)-, Wherein X Is Chalcogen, Attached Directly Or Indirectly To The Oxazole Ring By Nonionic Bonding Patents (Class 548/236)
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Publication number: 20130231375Abstract: The present invention relates to N-cycloalkyl-N-biphenylmethyl-carboxamide derivatives of formula (I) wherein A, Z1, Z2, Z3, X, n, Y and m represent various substituents, their process of preparation, preparation intermediate compounds, their use as fungicide active agents, particularly in the form of fungicide compositions and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.Type: ApplicationFiled: July 30, 2009Publication date: September 5, 2013Inventors: Philippe Desbordes, Ralf Dunkel, Stephanie Gary, Marie-Claire Grosjean-Cournoyer, Benoit Hartmann, Philippe Rinolfi, Jean-Pierre Vors, Rachel Rama
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Publication number: 20130231319Abstract: The invention relates to a method for preparing linear polymers having an amide end or having a star architecture comprising an amide core, by means of a ring opening using lactide and glycolide monomers or a lactide monomer ring in the presence of a catalyst, wherein the method includes the steps of: (i) reacting the excess monomer(s) with an initiator in a solvent, said initiator being selected from among an amine and an amino alcohol, given that the initiator has at least one primary or secondary amine function; (ii) adding a catalyst, said catalyst being a non-nucleophilic base and including at least one neutral sp2 nitrogen atom; and (iii) neutralizing the reaction mixture. Said novel method is particularly advantageous in that it can be easily monitored and enables better modulation of the polymers, and thus of the properties thereof, than the methods of the prior art. The invention also relates to novel polymers that are obtainable by means of said method.Type: ApplicationFiled: November 16, 2011Publication date: September 5, 2013Applicant: Actelion Pharmaceuticals Ltd.Inventors: Daniel Bur, Olivier Corminboeup, Sylvaine Gren, Corinna Grisostomi, Xavier Leroy, Sylvia Richard-Bildstein, Davide Pozzi
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Publication number: 20130225644Abstract: Lysine mimetic compounds having useful pharmacological activity such as antiarrhythmic activity and desirable bioavailability properties are disclosed.Type: ApplicationFiled: April 1, 2013Publication date: August 29, 2013Applicant: Zealand Pharma A/SInventor: Zealand Pharma A/S
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Publication number: 20130224186Abstract: Disclosed are new substituted oxazole and thiazole compounds of Formula (I) and pharmaceutically acceptable salts, esters or prodrugs thereof, compositions of the derivatives together with pharmaceutically acceptable carriers, and uses thereof:Type: ApplicationFiled: April 13, 2011Publication date: August 29, 2013Inventors: Paul A. Barsanti, Yu Ding, Wooseok Han
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Patent number: 8519137Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: GrantFiled: October 10, 2008Date of Patent: August 27, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Pramod Joshi, Paul Krenitsky, Andreas Termin, Dean Wilson
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Publication number: 20130211087Abstract: The present invention is directed to 7-aza-spiro[3.5]nonane-7-carboxylate derivatives of the Formula I. The compounds of the invention are inhibitors of the enzyme Fatty Acid Amide Hydrolase (FAAH). The invention also relates to processes for the preparation of compounds of the Formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.Type: ApplicationFiled: January 28, 2013Publication date: August 15, 2013Applicant: SANOFIInventors: Ahmed ABOUABDELLAH, Nathalie CHEREZE, Aude FAYOL, Alistair LOCHEAD, Mourad SAADY, Julien VACHE, Philippe YAICHE
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Patent number: 8501933Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is a group of formula A or formula B, and X, R2, R3, R4, R5, R6, Ra and Rb are as defined herein. Also provided are methods of using the compounds for treating diseases mediated by a P2X3 and/or a P2X2/3 receptor antagonist and methods of making the subject compounds.Type: GrantFiled: July 26, 2010Date of Patent: August 6, 2013Assignee: Roche Palo Alto LLCInventors: Li Chen, Michael Patrick Dillon, Lichun Feng, Ronald Charles Hawley, Minmin Yang
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Publication number: 20130197011Abstract: Substituted phenyl-3-aza-bicyclo[3.1.0]hex-3-yl-methanones which are glycine transporter-1 (GlyT1) inhibitors. These are useful for the treatment of schizophrenia, Alzheimer's Disease and other neurological and psychiatric disorders.Type: ApplicationFiled: July 27, 2012Publication date: August 1, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Riccardo GIOVANNINI, Barbara BERTANI, Marco FERRARA, Iain LINGARD, Rocco MAZZAFERRO, Holger ROSENBROCK
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Publication number: 20130190330Abstract: The present application relates to novel bisaryl-linked 5-aryl-1,2,4-triazolone derivatives, to processes for preparing them, to their use alone or in combinations for the treatment and/or prevention of diseases and also to their use for the production of medicaments for the treatment and/or prevention of diseases, more particularly for the treatment and/or prevention of cardiovascular disorders.Type: ApplicationFiled: February 25, 2011Publication date: July 25, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Chantal Furstner, Joerg Keldenich, Martina Delbeck, Peter Kolkhof, Axel Kretschmer, Ingo Pluschkell, Elisabeth Pook, Carsten Schmeck, Hubert Trubel
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Publication number: 20130184468Abstract: The invention relates to a process for the preparation of a compound of formula (I) or a salt thereof.Type: ApplicationFiled: March 11, 2013Publication date: July 18, 2013Applicant: Hoffmann-La Roche Inc.Inventor: Hoffmann-La Roche Inc.
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Publication number: 20130172316Abstract: The invention relates to new azetidine derivatives of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.Type: ApplicationFiled: December 14, 2012Publication date: July 4, 2013Inventors: Martin FLECK, Bernd NOSSE, Gerald Juergen ROTH
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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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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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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: 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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Patent number: 8450496Abstract: The invention relates to a process for the preparation of a compound of formula (I) or a salt thereof.Type: GrantFiled: March 17, 2010Date of Patent: May 28, 2013Assignee: Hoffman-La Roche Inc.Inventors: Kurt Puentener, Michelangelo Scalone
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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: 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: 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: 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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Publication number: 20130085276Abstract: The use of a complex of the form Z—M—OR in the carboxylation of a substrate is described. The group Z is a two-electron donor ligand, M is a metal and OR is selected from the group consisting of OH, alkoxy and aryloxy. The substrate may be carboxylated at a C—H or N—H bond. The metal M may be copper, silver or gold. The two-electron donor ligand may be a phosphine, a carbene or a phosphite ligand. Also described are methods of manufacture of the complexes and methods for preparing isotopically labelled caboxylic acids and carboxylic acid derivatives.Type: ApplicationFiled: June 9, 2011Publication date: April 4, 2013Inventors: Steven P. Nolan, Catherine Cazin
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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: 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: 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: 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: 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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Patent number: 8378095Abstract: 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 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: GrantFiled: May 9, 2008Date of Patent: February 19, 2013Assignee: Saruem LimitedInventors: John Charles Reader, John Mark Ellard, Michael Cherry
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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: 8372984Abstract: In one aspect, the invention relates to compounds having the formula: wherein: Ar, Z, R3, R4 and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: GrantFiled: July 14, 2010Date of Patent: February 12, 2013Assignee: Theravance, Inc.Inventors: Paul R. Fatheree, Ryan Hudson, Robert Murray McKinnell
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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: 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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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: 20130011361Abstract: The present invention provides heterocyclic derivatives of formula (I) that 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: October 1, 2010Publication date: January 10, 2013Applicants: XENON PHARMACEUTICALS INC., NOVARTIS AGInventors: Natalie Dales, Jianmin Fu, Qi Jia, Natalia Pokrovskaia, Shaoyi Sun, Zaihui Zhang
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Publication number: 20130012540Abstract: This disclosure concerns novel compounds of Formula (I) or as defined in the specification and compositions comprising such novel compounds. These compounds are useful antiviral agents, especially in inhibiting the function of the NS5A protein encoded by Hepatitis C virus (HCV). Thus, the disclosure also concerns a method of treating HCV related diseases or conditions by use of these novel compounds or a composition comprising such novel compounds.Type: ApplicationFiled: September 12, 2012Publication date: January 10, 2013Inventors: Rico Lavoie, John A. Bender, Jeffrey Lee Romine, Edward H. Ruediger, Carol Bachand, Omar D. Lopez, Qi Chen, Makonen Belema, John F. Kadow, Lawrence G. Hamann
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Publication number: 20130012513Abstract: Described herein are compounds, pharmaceutical compositions and methods for the inhibition of Hedgehog signaling. Said compounds, pharmaceutical compositions and methods have utility in the treatment of human and veterinary disease and disorders.Type: ApplicationFiled: January 6, 2011Publication date: January 10, 2013Inventors: Jean-Michel Vernier, John May, Patrick O'Connor, William Ripka, Anthony Pinkerton, Pierre-Yves Bounaud, Stephanie Hopkins
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Publication number: 20130012514Abstract: Aminoalkyloxazole and aminoalkylthiazolecarboxylic acid amides of formulae (1) and (2) where X represents O or S, Y represents C or N, where the two atoms must be different from one another, R2 represents hydrogen or acyl and R1 and R3, which may be identical or different, represent a substituent selected from the group consisting of branched or straight-chain, substituted or unsubstituted alkyl groups, alkylcycloalkyl groups, alkylaryl groups, cycloalkyl groups, cycloalkylaryl groups, aryl groups and arylcycloalkyl groups which optionally contain heteroatoms, a pharmaceutically acceptable salt, a stereoisomer, a stereoisomer mixture, a tautomer or a prodrug compound, preferably a prodrug ester and a prodrug peptide, thereof.Type: ApplicationFiled: February 4, 2011Publication date: January 10, 2013Applicant: EMC microcollections GmbHInventors: Holger Eickhoff, Hubert Löwenheim
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Publication number: 20130005730Abstract: The present invention relates to certain novel 1,3-oxazolidine compounds of formula (I), to processes for making such compounds and to their utility as renin inhibitors or prodrugs of renin inhibitors.Type: ApplicationFiled: October 29, 2010Publication date: January 3, 2013Inventors: Piaoyang Sun, Mikhajlovich Antonov Dmitry, Xiao Xiong Zhou
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Publication number: 20130005663Abstract: The present invention is directed to a compound of the formula: or pharmaceutically acceptable salts thereof and use of such compounds for treating proliferative diseases such as cancer, in mammals.Type: ApplicationFiled: September 7, 2012Publication date: January 3, 2013Applicant: NOVARTIS AGInventors: Mark G. CHAREST, Christine Hiu-Tung CHEN, Zhuoliang CHEN, Miao DAI, Feng HE, Huangshu LEI, Ly Luu PHAM, Sushil Kumar SHARMA, Christopher Sean STRAUB, Run-Ming David WANG, Fan YANG, Leigh ZAWEL
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Patent number: 8343970Abstract: Compounds that inhibit PDE10 are disclosed that have utility in the treatment of a variety of conditions, including (but not limited to) psychotic, anxiety, movement disorders and/or neurological disorders such as Parkinson's disease, Huntington's disease, Alzheimer's disease, encephalitis, phobias, epilepsy, aphasia, Bell's palsy, cerebral palsy, sleep disorders, pain, Tourette's syndrome, schizophrenia, delusional disorders, drug-induced psychosis and panic and obsessive-compulsive disorders. Pharmaceutically acceptable salts, stereoisomers, solvates and prodrugs of the compounds are also provided. Also disclosed are compositions containing a compound in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting PDE10 in a warm-blooded animal in need of the same.Type: GrantFiled: March 10, 2011Date of Patent: January 1, 2013Assignee: Omeros CorporationInventors: Neil S. Cutshall, Jennifer Lynn Gage, Thomas Neil Wheeler, Thomas L. Little
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Patent number: 8329913Abstract: An object of the present invention is to provide novel carbazole derivatives, solvates thereof, or pharmaceutically acceptable salts thereof having an excellent adipose tissue weight reducing effect, hypoglycemic effect, and hypolipidemic effect, which are useful as a preventive and/or therapeutic agent for fatty liver, obesity, lipid metabolism abnormality, visceral adiposity, diabetes, hyperlipemia, impaired glucose tolerance, hypertension, non-alcoholic fatty liver disease, non-alcoholic steatohepatitis, and the like.Type: GrantFiled: October 28, 2005Date of Patent: December 11, 2012Assignee: Zeria Pharmaceutical Co., Ltd.Inventors: Masakazu Murata, Yoshihiko Itokazu, Ryu Nakao
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Publication number: 20120309724Abstract: In one aspect, the invention relates to compounds having the formula: where R1, R2, R3, X, R4, R5, and R6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: ApplicationFiled: May 18, 2012Publication date: December 6, 2012Applicant: THERAVANCE, INC.Inventors: Melissa Fleury, Roland Gendron, Adam D. Hughes, Jane Schmidt
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Publication number: 20120309738Abstract: This invention relates to compounds of formula I their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), to pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions. A, M, W, R1, R2, R3, R4, R6, R2, R7, R8, R9, Ra, Rb have meanings given in the description.Type: ApplicationFiled: December 8, 2011Publication date: December 6, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Henning Priepke, Raimund Kuelzer, Juergen Mack, Roland Pfau, Dirk Stenkamp, Benjamin Pelcman, Robert Roenn, Dimitrijs Lubriks, Edgars Suna
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Publication number: 20120302607Abstract: The invention provides a series of C4-substituted oxazole compounds having an alpha keto side chain at the 2 position, for example, compounds of formula I. The compounds can inhibit fatty acid amide hydrolase and can be useful for treatment of malconditions modulated by fatty acid amide hydrolase. The invention further provides methods of making compounds of formula I, useful intermediates in the preparation of compounds of formula I, and methods of using compounds of formula 1 and compositions thereof.Type: ApplicationFiled: August 2, 2012Publication date: November 29, 2012Applicant: The Scripps Research InstituteInventor: Dale L. Boger
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Publication number: 20120302562Abstract: Compounds that may be used to inhibit Notum Pectinacetylesterase are described, as well as compositions comprising them, and methods of their use to treat diseases and disorders affecting bone.Type: ApplicationFiled: May 23, 2012Publication date: November 29, 2012Inventors: Joseph BARBOSA, Kenneth Gordon CARSON, Michael Walter GARDYAN, Jason Patrick HEALY, Qiang HAN, Ross MABON, Praveen PABBA, James TARVER, JR., Kristen M. TERRANOVA, Ashok TUNOORI, Xiaolian XU
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Publication number: 20120295923Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.Type: ApplicationFiled: January 19, 2011Publication date: November 22, 2012Inventors: Christopher William Am Ende, Benjamin Adam Fish, Douglas Scott Johnson, Ricardo Lira, Christopher John O'Donnell, Martin Youngjin Pettersson, Corey Michael Stiff
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Publication number: 20120295894Abstract: Described herein are novel beta-secretase inhibitors and methods for their use, including methods of treating Alzheimer's disease.Type: ApplicationFiled: December 1, 2011Publication date: November 22, 2012Inventors: Geoffrey M. BILCER, Thippeswamy Devasamudram, Sudha V. Ankala, John C. Lilly, Chunfeng Liu, Hui Lei, Arun K. Ghosh, Makoto Inoue