Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To Ring Carbon Of The Oxazole Ring By Nonionic Bonding Patents (Class 548/248)
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Patent number: 8623860Abstract: 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: GrantFiled: December 14, 2012Date of Patent: January 7, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Martin Fleck, Bernd Nosse, Gerald Juergen Roth
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Patent number: 8618138Abstract: This invention provides novel compounds and the novel compounds for use as a medicine, more in particular for the prevention or treatment of neurodegenerative disorders, more specifically certain neurological disorders, such as disorders collectively known as tauopathies, and disorders characterized by cytotoxic ?-synuclein amyloidogenesis. The present invention also relates to the use of said novel compounds for the manufacture of medicaments useful for treating such neurodegenerative disorders. The present invention further relates to pharmaceutical compositions including said novel compounds and to methods for the preparation of said novel compounds.Type: GrantFiled: June 11, 2010Date of Patent: December 31, 2013Assignees: Katholieke Universiteit Leuven, K.U. Leuven R&D, reMYNDInventors: Gerard Griffioen, Tom Van Dooren, Veronica Rojas De La Parra, Arnaud Marchand, Sara Allasia, Amuri Kilonda, Patrick Chaltin
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Publication number: 20130330366Abstract: In one aspect, the invention relates to compounds having the formula XII: where Ra, Rb, R2, R7, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds described herein are prodrugs of compounds having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.Type: ApplicationFiled: June 6, 2013Publication date: December 12, 2013Inventors: Adam D. Hughes, Melissa Fleury
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Publication number: 20130330365Abstract: In one aspect, the invention relates to compounds having the formula X: where Ra, Rb, R2, R7, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds described herein are prodrugs of compounds having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.Type: ApplicationFiled: June 6, 2013Publication date: December 12, 2013Inventors: Adam D. Hughes, Melissa Fleury
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Patent number: 8592456Abstract: The present invention relates to compounds of the general formula (I), and the pharmaceutically acceptable salt or solvate thereof, as anti-inflammatory and immunomodulatory agents.Type: GrantFiled: January 27, 2012Date of Patent: November 26, 2013Assignee: 4SC Discovery GmbHInventors: Johann Leban, Stefan Tasler, Roland Baumgartner, Wael Saeb, Carine Chevrier
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Publication number: 20130310377Abstract: Disclosed are novel calcium release-activated calcium (CRAC) channel inhibitors, methods for preparing them, pharmaceutical compositions containing them, and methods of treatment using them. The present disclosure also relates to methods for treating non-small cell lung cancer (NSCLC) with CRAC inhibitors, and to methods for identifying therapeutics for treating and of diagnosing cancer.Type: ApplicationFiled: December 20, 2012Publication date: November 21, 2013Applicant: Rhizen Phamaceuticals SAInventor: Rhizen Phamaceuticals SA
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Patent number: 8586571Abstract: The present invention relates to wherein each symbol is as defined in the specification. The compound of the present invention has a superior RBP4-lowering action, and is useful as a medicament for the prophylaxis or treatment of disease and condition mediated by increased RBP4.Type: GrantFiled: October 17, 2008Date of Patent: November 19, 2013Assignee: Takeda Pharmaceutical Company LimitedInventors: Shizuo Kasai, Tomohiro Kaku, Masahiro Kamaura
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Publication number: 20130295261Abstract: The present invention provides isosorbide derivatives having the formula shown below and certain subgenera or species thereof, as flavor or taste modifiers, particularly, savory (“umami”) taste modifiers, savory flavoring agents and savory flavor enhancers in foods, beverages, and other comestible compositions,Type: ApplicationFiled: March 13, 2013Publication date: November 7, 2013Applicant: SENOMYX, INC.Inventors: Catherine TACHDJIAN, Donald S. Karanewsky, Sara L. Adamski-Werner, Jeffrey M. Yamamoto, Guy Servant
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Publication number: 20130281387Abstract: Provided herein are methods for treating conditions associated with a chemosensory receptor, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administering a composition comprising a chemosensory receptor ligand. Also provided herein are chemosensory receptor ligand compositions and methods for the preparation thereof for use in the methods of the present invention.Type: ApplicationFiled: October 18, 2011Publication date: October 24, 2013Applicant: ELCELYX THERAPEUTICS, INC.Inventors: Alain D. Baron, Martin R. Brown, Christopher R.G. Jones, Nigel R.A. Beeley
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Patent number: 8563714Abstract: The present invention relates to bridged spiro[2.4]heptane derivatives of formula (I), wherein W, Y, Z, R1 and R2 are as defined in the description, their preparation and their use as pharmaceutically active compounds as ALX receptor and/or FPRL2 agonists for the treatment of inflammatory and obstructive airways diseases.Type: GrantFiled: May 17, 2010Date of Patent: October 22, 2013Assignee: Actelion Pharmaceuticals Ltd.Inventors: Daniel Bur, Olivier Corminboeuf, Sylvaine Cren, Corinna Grisostomi, Xavier Leroy, Sylvia Richard-Bildstein
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Publication number: 20130274301Abstract: The invention relates to the use of polycycloolefins in electronic devices and more specifically to the use of such polycycloolefins as interlayers applied to insulating layers used in electronic devices, the electronic devices that encompass such polycycloolefin interlayers and processes for preparing such polycycloolefin interlayers and electronic devices.Type: ApplicationFiled: August 23, 2011Publication date: October 17, 2013Applicant: AL-GIAX PHARMACEUTICALS GMBHInventors: Guido Koopmans, Birgit Hasse, Stefan Mullner
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Publication number: 20130261133Abstract: The compounds of the invention exhibit antiprotozoal, antimicrobial, and anticancer properties that are useful for the treatment or prevention of infections or cancer in a patient (e.g., a human). For example, the compounds and methods described herein can be used for the treatment or prevention of protozoal infections such as leishmaniasis, malaria, and trypanosoma infections, bacterial infections such as S. aureus and C. albicans, and cancers such as breast, colon, lung, or prostate cancer. The invention further provides methods of synthesizing such compounds as well as kits useful for administering the compounds.Type: ApplicationFiled: March 14, 2013Publication date: October 3, 2013Applicant: The University of MontanaInventors: John Howard Hoody, David Brian Bolstad
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Publication number: 20130261158Abstract: The present invention relates to fungicide N-(2-phenoxyethyl)carboxamide derivatives of formula (I), their aza, thia and sila analogues, their process of preparation, their use as fungicides, particularly in the form of fungicidal compositions and methods for the control of phytopathogenic fungi of plants using these compounds or their compositions. Formula (1) wherein A, T, W, X, n and Z3 to Z7 represent various substituents.Type: ApplicationFiled: July 30, 2009Publication date: October 3, 2013Inventors: Samir Bennabi, Jurgen Benting, Stephane Brunet, Philippe Desbordes, Peter Dahmen, Stephanie Gary, Marie-Claire Grosjean-Cournoyer, Rachel Rama, Philippe Rinolfi, Valerie Toquin, Arnd Voerste, Ulrike Wachendorff-Neumann
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Patent number: 8530465Abstract: The invention provides a series of novel 1,2-disubstituted amido-anthraquinone derivatives. Further, the invention also provides the preparation method and application of said derivatives, said application comprises: said derivatives with therapeutically effective amount are prepared into pharmaceutical compositions for inhibition of cancer cell growth, further treating cancer.Type: GrantFiled: August 1, 2012Date of Patent: September 10, 2013Assignee: National Defense Medical CenterInventors: Hsu-Shan Huang, Chia-Chung Lee
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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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Publication number: 20130203709Abstract: The present disclosure relates to acylsulfonamides and processes for their preparation. The processes involve a target-guided synthesis approach, whereby a thioacid and a sulfonyl azide are reacted in the presence of a biological target protein, a Bcl-2 family protein, to form the acylsulfonamide.Type: ApplicationFiled: August 9, 2011Publication date: August 8, 2013Applicants: THE PENN STATE RESEARCH FOUNDATION, UNIVERSITY OF SOUTH FLORIDAInventors: Roman Manetsch, Sameer Kulkarni, Iredia D. Iyamu, Hong-Gang Wang, Kenichiro Doi, Wayne Guida, Daniel Santiago, Courtney du Boulay
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Patent number: 8492365Abstract: The present invention pertains, at least in part, to novel 7-substituted tetracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for minocycline and tetracycline compounds in general, such as blocking tetracycline efflux and modulation of gene expression.Type: GrantFiled: June 9, 2009Date of Patent: July 23, 2013Assignees: Trustees of Tufts College, Paratek Pharmaceuticals, Inc.Inventors: Mark L. Nelson, Roger Frechette, Peter Viski, Mohamed Ismail, Todd Bowser, Beena Bhatia, David Messersmith, Laura McIntyre, Darrell Koza, Glen Rennie, Paul Sheahan, Paul Hawkins, Atul Verma, Tadeusz Warchol, Upul Bandarage
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Publication number: 20130184315Abstract: Compounds of formula (I) and formula (II) 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: July 18, 2011Publication date: July 18, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GmbHInventors: Eugene Richard Hickey, Doris Riether, Monika Ermann
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Publication number: 20130184222Abstract: Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1 comprising administering to a subject in need thereof a compound described here.Type: ApplicationFiled: July 15, 2011Publication date: July 18, 2013Applicant: AGIOS PHARMACEUTICALS, INCInventors: Janeta Popovici-Muller, Francesco G. Salituro, Jeffrey Saunders, Jeremy Travins, Shunqi Yan
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Publication number: 20130178506Abstract: The present invention relates to compounds and methods for inducing synthesis and secretion of insulin from pancreatic beta cells. The methods may take place in vitro, ex vivo such as in isolates from adult mammalian tissue, or in vivo. Compounds and methods described herein may find use in the treatment of diabetes.Type: ApplicationFiled: November 21, 2012Publication date: July 11, 2013Applicant: The Board of Regents of the University of Texas SystemInventor: The Board of Regents of the University of Texas S
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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: 20130158004Abstract: Azetidine derivatives of which the following is exemplary and their use in the treatment of obesity, diabetes or dyslipidemia.Type: ApplicationFiled: December 14, 2012Publication date: June 20, 2013Inventors: Martin FLECK, Bernd NOSSE, Niklas HEINE, Gerald Juergen ROTH
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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: 20130131321Abstract: The present invention relates to the use for affinity purification of an antibody or an fragment of an antibody, of a ligand-substituted matrix comprising a support material and at least one ligand covalently bonded to the support material, the ligand being represented by formula (I) wherein Sp is a spacer group; v is 0 or 1; Am is an amide group —NR1—C(O)—, and wherein either NR1 is attached to Ar1 and —C(O)— is attached to Ar2, or —C(O)— is attached to Ar1 and NR1 is attached to Ar2; and R1 is hydrogen or C1 to C4 alkyl, preferably hydrogen or methyl; and more preferably hydrogen; Ar1 is a divalent 5- or 6-membered substituted or unsubstituted aromatic ring; Ar2 is 5- or 6-membered heterocyclic aromatic ring which is (a) attached to a further 5- or 6-membered aromatic ring via a single bond; or (b) fused to a further 5- or 6-membered aromatic ring as part of a multicyclic ring system; or (c) attached to at least one substituent selected from C1 to C4 alkyl; C2 to C4 alkenyl; C2 to C4 alkynyl; aType: ApplicationFiled: August 3, 2011Publication date: May 23, 2013Applicant: GRAFFINITY PHARMACEUTICALS GMBHInventors: Holger Bittermann, Klaus Burkert, Marc Arnold, Oliver Keil, Thomas Neumann, Inge Ott, Kristina Schmidt, Daniel Schwizer, Renate Sekul
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Publication number: 20130116240Abstract: Provided is an agent for the treatment or prophylaxis of inflammatory diseases, allergic diseases, autoimmune diseases, transplant rejection or the like. A compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, or a solvate thereof: wherein each symbol is as described in the specification.Type: ApplicationFiled: September 26, 2012Publication date: May 9, 2013Applicant: JAPAN TOBACCO INC.Inventor: Japan Tobacco Inc.
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Patent number: 8420145Abstract: The present invention provides isosorbide derivatives having the formula shown below and certain subgenera or species thereof, as flavor or taste modifiers, particularly, savory (“umami”) taste modifiers, savory flavoring agents and savory flavor enhancers in foods, beverages, and other comestible compositions,Type: GrantFiled: March 3, 2009Date of Patent: April 16, 2013Assignee: Senomyx, Inc.Inventors: Catherine Tachdjian, Donald S. Karanewsky, Sara L. Adamski-Werner, Jeffrey M. Yamamoto, Guy Servant
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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: 20130065877Abstract: The present disclosure relates to a series of substituted phenyl cycloalkyl pyrrolidine (piperidine) spirolactams and amides of formula (Ia) and formula (Ib). wherein R1, R2, R3, R4, X, m, l, n, p and s are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this disclosure relates to methods of preparation of substituted phenyl cycloalkyl pyrrolidine (piperidine) spirolactams and amides of formula (Ia) and (Ib), and intermediates therefor.Type: ApplicationFiled: November 6, 2012Publication date: March 14, 2013Applicant: SANOFIInventor: SANOFI
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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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Novel 1, 2-Disubstituted Amido-anthraquinone Derivatives, Preparation Method and application thereof
Publication number: 20130059862Abstract: The invention provides a series of novel 1,2-disubstituted amido-anthraquinone derivatives. Further, the invention also provides the preparation method and application of said derivatives, said application comprises: said derivatives with therapeutically effective amount are prepared into pharmaceutical compositions for inhibition of cancer cell growth, further treating cancer.Type: ApplicationFiled: August 1, 2012Publication date: March 7, 2013Inventor: Hsu-Shan HUANG -
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: 20130017196Abstract: The present invention relates to new substituted imidazole compounds and pharmaceutically acceptable salts, esters or prodrugs thereof, compositions of the new compounds together with pharmaceutically acceptable carriers, and uses of the new compounds.Type: ApplicationFiled: September 13, 2012Publication date: January 17, 2013Inventors: Weibo Wang, Paul A. Barsanti, Yia Xia, Rustum Boyce, Sabina Pecchi, Nathan Brammeier, Megan C. Phillips, Kris Mendenhall, Kelly Wayman, Liana Marie Lagnition, Ryan Constantine, Hong Yang, Elizabeth Mieuli, Savithri Ramurthy, Elisa Jazan, Anu Sharma, Rama Jain, Sharadha Subramanian, Paul A. Renhowe, Kenneth W. Bair, David Duhl, Annette Walter, Tinya Abrams, Kay Huh, Eric Martin, Mark Knapp, Vincent P. Le
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Publication number: 20130012708Abstract: A compound represented by the formula (1): wherein A is a nitrogen atom or CR4, B is an oxygen atom, a sulfur atom or NR9 (provided that when A is a nitrogen atom, B is not NH), R1 is a C2-14 aryl group, L1 is a bond, CR10R11, an oxygen atom, a sulfur atom or NR12, X is OR13, SR13 or NR14NR15, R2 is a hydrogen atom, a formyl group, a C1-10 alkyl group or the like, L2 is a bond or the like, L3 is a bond, CR17R18, an oxygen atom, a sulfur atom or NR19, L4 is a bond, CR20R21, an oxygen atom, a sulfur atom or NR22, Y is an oxygen atom, a sulfur atom or NR23, and R3 is a C2-14 aryl group, a tautomer, prodrug or pharmaceutically acceptable salt of the compound or a solvate thereof.Type: ApplicationFiled: September 13, 2012Publication date: January 10, 2013Applicant: Nissan Chemical Industries LimitedInventors: Shingo Owada, Shunsuke Iwamoto, Kazufumi Yanagihara, Katsuaki Miyaji, Takanori Nakamura, Norihisa Ishiwata, Yutaka Hirokawa
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Publication number: 20130005782Abstract: This invention relates generally to integrin ligand discovery and to a method of integrin ligand discovery base upon induction of ligand-induced epitopes. Such ligands have the potential to be active agent as anti-inflammatory, anti-angiogenesis and/or anti-thrombotic agents and for the treatment of integrin mediated diseases and/or conditions.Type: ApplicationFiled: March 23, 2011Publication date: January 3, 2013Inventors: Alexandre Chigaev, Larry A. Sklar
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Publication number: 20120322787Abstract: A compound is represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating a subject in need thereof comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. The subject has type 2 diabetes; renal hypertrophy or hyperplasia associated with diabetic nephropathy; Tay-Sachs; Gaucher's; or Fabry's disease. Methods of decreasing plasma TNF-?, lowering blood glucose levels, decreasing glycated hemoglobin levels, inhibiting glucosylceramide synthase, and lowering glycosphingolipid concentrations in a subject in need thereof respectively comprise administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: August 27, 2012Publication date: December 20, 2012Applicant: Genzyme CorporationInventors: Craig Siegel, Cecilia M. Bastos, David J. Harris, Angeles Dios, Edward Lee, Richard Silva, Lisa M. Cuff, Mikaela Levine, Cassandra A. Celatka, Frederic Vinick, Thomas H. Jozefiak, Yibin Xiang, John Kane, Junkai Liao
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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: 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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Patent number: 8318750Abstract: A compound of formula (I) or stereoisomers or pharmaceutically acceptable salts thereof, and their preparation and use as pharmaceuticals wherein R1, R2 and R3 are as defined herein.Type: GrantFiled: August 26, 2011Date of Patent: November 27, 2012Assignee: Novartis AGInventors: Robin Alec Fairhurst, Roger John Taylor, Brian Cox
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Patent number: 8318951Abstract: The present invention relates to screens for compounds that can induce stem cell differentiation. In addition, isoxazoles and sulfonyl hydrazones are identified as general classes of compounds that can induce differentiation of stem cells into cells of neuronal and cardiac fate, respectively.Type: GrantFiled: May 26, 2011Date of Patent: November 27, 2012Assignee: The Board of Regents of the University of Texas SystemInventors: Eric N. Olson, Douglas Frantz, Jenny Hsieh, Steven L. McKnight, Jay Schneider
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Publication number: 20120295938Abstract: The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, blood clot formation, asthma or symptoms thereof, agitation or a symptom thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like.Type: ApplicationFiled: March 9, 2012Publication date: November 22, 2012Inventors: BRADLEY TEEGARDEN, DENNIS CHAPMAN, MARC DECAIRE, PETER I. DOSA, KONRAD FEICHTINGER, HONNAPPA JAYAKUMAR, THUY-ANH TRAN, SONJA STRAH-PLEYNET, JAY XU
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Publication number: 20120270861Abstract: The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggreagation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, blood clot formation, asthma or symptoms thereof, agitation or a symptom thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like.Type: ApplicationFiled: March 9, 2012Publication date: October 25, 2012Inventors: BRADLEY TEEGARDEN, DENNIS CHAPMAN, JUYI CHOI, KONRAD FEICHTINGER, SANGDON HAN, HONNAPPA JAYAKUMAR, THUY-AND TRAN, JINGDONG XU, NING ZOU
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Publication number: 20120259113Abstract: 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: ApplicationFiled: January 9, 2012Publication date: October 11, 2012Applicant: THERAVANCE, INC.Inventors: Brooke Blair, Paul R. Fatheree, Melissa Fleury, Roland Gendron, Ryan Hudson, Robert Murray McKinnell, Michael Wilson
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Patent number: 8283383Abstract: 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: GrantFiled: June 22, 2010Date of Patent: October 9, 2012Assignee: Roche Palo Alto LLCInventors: Chris Allen Broka, Ronald Charles Hawley
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Publication number: 20120252770Abstract: Compounds of formula (I): The present invention relates to novel indazolyl ester or amide derivatives, to pharmaceutical compositions comprising such derivatives, to processes for preparing such novel derivatives and to the use of such derivatives as medicamentsType: ApplicationFiled: March 23, 2012Publication date: October 4, 2012Inventors: Markus Berger, Jan Dahmén, Karl Edman, Anders Eriksson, Balint Gabos, Thomas Hansson, Martin Hemmerling, Krister Henriksson, Svetlana Ivanova, Matti Lepistö, Darren McKerrencher, Magnus Munck af Rosenschöld, Stinabritt Nilsson, Hartmut Rehwinkel, Camilla Taflin
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Patent number: 8258141Abstract: A compound of formula (I) or stereoisomers or pharmaceutically acceptable salts thereof, and their preparation and use as pharmaceuticals wherein R1, R2 and R3 are as defined herein.Type: GrantFiled: April 19, 2007Date of Patent: September 4, 2012Assignee: Novartis AGInventors: Robin Alec Fairhurst, Roger John Taylor, Brian Cox
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Publication number: 20120214786Abstract: This invention relates to compounds of formula I their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), 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, R6, R7, R8 have meanings given in the description.Type: ApplicationFiled: August 17, 2011Publication date: August 23, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Henning PRIEPKE, Henri DOODS, Raimund KUELZER, Roland PFAU, Dirk STENKAMP, Benjamin PELCMAN, Robert ROENN
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Publication number: 20120196862Abstract: The present invention relates to compounds of the general formula (I), and the pharmaceutically acceptable salt or solvate thereof, as anti-inflammatory and immunomodulatory agents.Type: ApplicationFiled: January 27, 2012Publication date: August 2, 2012Applicant: 4SC Discovery GmbHInventors: Johann LEBAN, Stefan TASLER, Wael SAEB, Carine CHEVRIER
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Publication number: 20120196861Abstract: The present invention relates to compounds of the general formula (I), and the pharmaceutically acceptable salt or solvate thereof, as anti-inflammatory and immunomodulatory agents.Type: ApplicationFiled: January 27, 2012Publication date: August 2, 2012Applicant: 4SC Discovery GmbHInventors: Johann LEBAN, Stefan TASLER, Roland BAUMGARTNER, Wael SAEB, Carine CHEVRIER
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Patent number: 8227504Abstract: The present invention discloses and claims a series of substituted N-phenyl-pyrrolidinylmethylpyrrolidine amides of formula (I). Wherein R, R1, R2, R3 and R4 are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this invention also discloses methods of preparation of substituted pyrrolidinylmethylpyrrolidine amides and intermediates therefor.Type: GrantFiled: March 15, 2010Date of Patent: July 24, 2012Assignee: SanofiInventors: Werngard Czechtizky, Zhongli Gao, William Joseph Hurst, Lothar Schwink, Siegfried Stengelin