The Additional Hetero Ring Contains Nitrogen As The Only Ring Hetero Atom [e.g., 2-(2-imidazolin-2-yl)-benzimidazole; 1-p-chlorophenyl-3- Pyrrolidin-1- Yl-propyl Benzimidazolone, Etc.] Patents (Class 548/306.1)
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Publication number: 20130053403Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and methods of using the same in the treatment or prevention of diseases mediated by the activation of b3-adrenoceptor.Type: ApplicationFiled: April 25, 2011Publication date: February 28, 2013Inventors: Richard Berger, Scott D. Edmondson, Bart H. Harper
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Patent number: 8383832Abstract: Provided are methods for the synthesis of heterocyclic compounds such as benzimidazole carboxylic acid core structures having Formula Ib-1: wherein Z, X1, X2, X5, R2b and R10 are as defined herein. Compounds of Formula Ib-1 can be used to prepare heterocyclic derivatives such as benzimidazole derivatives.Type: GrantFiled: September 9, 2011Date of Patent: February 26, 2013Assignees: Array BioPharma Inc., AstraZeneca ABInventors: John Demattei, Sagar Shakya, Anthony D. Piscopio, Bruno P. Hache, Matthew Charles Evans, James Gair Ford, Simon Mark Pointon, Koen Peeters, Timothy John Lilley, John Leonard
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Publication number: 20130030004Abstract: The present invention relates to compounds of formula I: or a pharmaceutically acceptable salt thereof, that inhibit bacterial gyrase and/or TopoIV and pharmaceutically acceptable compositions comprising said compounds. These compounds, and compositions thereof, are useful in treating bacterial infection. Accordingly, the present invention also relates to methods for treating bacterial infections in mammals.Type: ApplicationFiled: November 6, 2006Publication date: January 31, 2013Inventors: Paul Charifson, David Deininger, Joseph Drumm, Anne-Laure Grillot, Arnaud LeTiran, Yusheng Liao, Emanuele Perola, Steven Ronkin, Dean Stamos, Tiansheng Wang
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Publication number: 20130023525Abstract: The present invention relates to compounds which inhibit bacterial gyrase and/or Topo IV and pharmaceutically acceptable compositions comprising said compounds. These compounds, and compositions thereof, are useful in treating bacterial infection. Accordingly, the present invention also relates to methods for treating bacterial infections in mammals.Type: ApplicationFiled: April 24, 2012Publication date: January 24, 2013Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Paul S. Charifson, David D. Deininger, Anne-Laure Grillot, Yusheng Liao, Steven Ronkin, Dean Stamos, Emanuele Perola, Tiansheng Wang, Arnaud Le Tiran, Joseph Drumm
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Publication number: 20130018039Abstract: Disclosed are compounds having the formula: wherein R1A, R1B, R2 and R3 are defined herein, and methods of making and using the same.Type: ApplicationFiled: March 31, 2011Publication date: January 17, 2013Inventors: Vera Q. Bodmer, Linda N. Casillas, Michael P. DeMartino, Philip A. Harris, Bryan W. King, Ami Lakdawala Shah, Lara Kathryn Leister, Joshi M. Ramanjulu, Joseph J. Romano, Gren Z. Wang, Matthew A. Wilson, David Duff Wisnoski
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Patent number: 8329737Abstract: A compound of the general formula (I) or pharmaceutically acceptable prodrugs, salts, hydrates, solvates, crystal forms or diastereomers thereof, wherein A represents a variety of six membered nitrogen containing heterocyclic rings, Q is a bond, halogen, C1-4 alkyl, O, S, SO2, CO or CS and X1, X2, X3 and X4 are optionally substituted by 9 specific substituents or one can be nitrogen. Compositions comprising a carrier and at least one compound of formula (I) are also provided. Further provided are methods of treating tyrosine kinase-associated disease states by administering a compound of formula (I) and methods of suppressing the immune system of a subject by administering a compound of formula (I).Type: GrantFiled: September 30, 2010Date of Patent: December 11, 2012Assignee: YM Biosciences Australia PTY LtdInventors: Michelle Leanne Styles, Jun Zeng, Herbert Rudolf Treutlein, Andrew Frederick Wilks, Marcel Robert Kling, Xianyong Bu, Christopher John Burns
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Patent number: 8329700Abstract: Pyrazine compounds of formula (I): or a pharmaceutically acceptable salt thereof, wherein m, n, p, R1, R2, R3, R4, X1, X2, X3, X4, X5, X6, X7, X8, X9, X10, X11, Y and Z are defined in the specification, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.Type: GrantFiled: March 7, 2011Date of Patent: December 11, 2012Assignee: Amgen Inc.Inventors: Jennifer R. Allen, Matthew Paul Bourbeau, Ning Chen, Essa Hu, Roxanne Kunz, Shannon Rumfelt
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Patent number: 8329899Abstract: Compounds of formula (I), pharmaceutical compositions comprising compounds of formula (I) and methods of inhibiting Hsp90 in a cell, treating or preventing a proliferation disorder in a mammal and treating cancer in a mammal comprising administering a compound of formula (I) to a patient or a cell. Variable R5 is an optionally substituted heteroaryl; an optionally substituted 6 to 14-membered aryl; a bicyclic 9-member heterocycle optionally substituted at any substitutable nitrogen or carbon atoms; or a substituent R18, defined herein. Ring A is an aryl or a heteroaryl optionally further substituted with one or more substituents in addition to R3. Substituent R3 is defined herein.Type: GrantFiled: February 14, 2011Date of Patent: December 11, 2012Assignee: Synta Pharmaceuticals, Corp.Inventors: Weiwen Ying, Shijie Zhang, Zhenjian Du, Kevin Foley
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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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Patent number: 8324219Abstract: This invention relates to certain biologically active chemical compounds, such as benzoimidazolyl-pyrazine derivatives of formula (I) or pharmaceutically acceptable salts thereof. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.Type: GrantFiled: September 19, 2008Date of Patent: December 4, 2012Assignee: Synta Pharmaceuticals Corp.Inventors: Shoujun Chen, Jun Jiang, Junyi Zhang, Lijun Sun
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Publication number: 20120301398Abstract: Radiolabeled glutaminylcyclase (QC) inhibitors as imaging agents, in particular, but not exclusively, as medical imaging agents for the detection of neurological disorders; and pharmaceutical compositions, methods and kits for detecting neurological disorders, using the radiolabeled inhibitors.Type: ApplicationFiled: May 24, 2012Publication date: November 29, 2012Applicant: PROBIODRUG AGInventors: Ulrich Heiser, Daniel Ramsbeck, Hans-Ulrich Demuth
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Publication number: 20120283260Abstract: The invention provides compositions and methods for treating and/or preventing ocular disorders associated with increased intraocular pressure. In particular, the compounds are bradykinin agonists.Type: ApplicationFiled: July 24, 2012Publication date: November 8, 2012Applicants: ASTELLAS PHARMA INC., ALCON RESEARCH, LTD.Inventors: Keith D. Combrink, Suchismita Mohapatra, Mark R. Hellberg, Najam A. Sharif, Ganesh Prasanna, Iok-Hou Pang, Bryon Severns, Hwang-Hsing Chen, Abdelmoula Namil
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Publication number: 20120283259Abstract: Novel heterocyclic derivatives 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: ApplicationFiled: July 12, 2012Publication date: November 8, 2012Applicant: PROBIODRUG AGInventors: Ulrich Heiser, Ulf-Torsten Gaertner, Hans-Ulrich Demuth
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Publication number: 20120276050Abstract: Clemizole and clemizole analog compounds, and pharmaceutical compositions of the same, are useful in methods of treating a host infected with a virus from the Flaviviridae family of viruses, methods of inhibiting HCV replication in a host, methods of inhibiting the binding of NS4B polypeptide to the 3?UTR of HCV negative strand RNA in a host, and methods of treating liver fibrosis in a host.Type: ApplicationFiled: March 16, 2010Publication date: November 1, 2012Inventors: Ingrid C. Choong, David Cory, Jeffrey S. Glenn, Wenjin Yang
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Publication number: 20120237475Abstract: Novel heterocyclic derivatives of formula (I): or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof, wherein Ra, n, R1 and R2 are as defined herein, as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5).Type: ApplicationFiled: March 16, 2012Publication date: September 20, 2012Applicant: PROBIODRUG AGInventors: Ulrich Heiser, Daniel Ramsbeck
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Publication number: 20120219594Abstract: Inhibitors of HCV replication of formula I including stereochemically isomeric forms, and salts, solvates thereof, wherein R and R? are, each independently, —CR1R2R3, aryl, heteroaryl or heteroC4-6cycloalkyl, whereby aryl and heteroaryl may optionally be substituted with 1 or 2 substituents selected from halo and methyl. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use in HCV therapy.Type: ApplicationFiled: November 3, 2010Publication date: August 30, 2012Inventors: Koen Vandyck, Stefaan Julien Last, Ioannis Nicolaos Houpis, Pierre Jean-Marie Bernard Raboisson
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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: 20120208821Abstract: Compounds are described herein useful for treating diseases and conditions by modulation of one or more alpha adrenergic receptor. The compounds can include a naphthalene, a quinoline, a benzoimidazole or an isoquinoline as a core structure. Methods of making, using and formulating these compounds are described.Type: ApplicationFiled: October 6, 2010Publication date: August 16, 2012Applicant: ALLERGAN, INCInventors: Ken Chow, Liming Wang, Wenkui K. Fang, Evelyn G. Corpuz, Santosh C. Sinha, Daniel W. Gil, Mohammad I. Dibas, John E. Donello
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Publication number: 20120208818Abstract: The present invention provides compounds of general formula I: or a pharmaceutically acceptable salt thereof, wherein X, n, Y, and R1 are defined generally and in subsets herein. Compounds of the invention are inhibitors of CCR2 and accordingly are useful for the treatment of a variety of inflammatory, allergic, and autoimmune diseases, disorders, or conditions.Type: ApplicationFiled: October 10, 2011Publication date: August 16, 2012Applicant: Millennium Pharmaceuticals, Inc.Inventors: Amy M. Elder, Shomir Ghosh, Sian Griffiths, Prakash Raman, Francois Soucy, Kevin Sprott, Qing Ye
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Publication number: 20120202856Abstract: The present invention is directed to benzimidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by TRP M8, including for example, inflammatory pain, inflammatory hyperalgesia, inflammatory hypersensitivity condition, neuropathic pain, neuropathic cold allodynia, inflammatory somatic hyperalgesia, inflammatory visceral hyperalgesia, cardiovascular disease aggravated by cold and pulmonary disease aggravated by cold.Type: ApplicationFiled: February 2, 2012Publication date: August 9, 2012Inventors: Mark R. PLAYER, Raul CALVO, Jinsheng CHEN, Carl ILLIG, Sanath MEEGALLA, Daniel PARKS, William PARSONS
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Publication number: 20120196897Abstract: The present invention relates to compounds of general formula I in which A, L, M, Q2, Q3, Q4, R1, R5, Ra, Rb, Rc, W, X, Y, Z1, Z2, Z3 are defined in the description, the salts thereof, particularly the physiologically acceptable salts thereof. The compounds are of potential utility in the treatment and/or prevention of inflammatory diseases and associated conditions, in particular, in the treatment and/or prevention of pain. The invention also relates to the use of such compounds as medicaments, to pharmaceutical compositions containing them, and to their preparation.Type: ApplicationFiled: April 6, 2012Publication date: August 2, 2012Applicant: Boehringer Ingelheim International GmbHInventors: Roland PFAU, Kirsten ARNDT, Henri DOODS, Klaus KLINDER, Raimund KUELZER, Dimitrijs LUBRIKS, Juergen MACK, Benjamin PELCMAN, Henning PRIEPKE, Robert ROENN, Dirk STENKAMP, Edgars SUNA
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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
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Publication number: 20120184535Abstract: A compound, a process for its preparation, a pharmaceutical composition, use of a compound, a method for modulating or regulating serine/threonine and tyrosine kinases and a serine/threonine and tyrosine kinases modulating agent. Novel small-molecule compounds with kinase inhibitory activity, having superior properties as pharmaceutical agents, production method thereof and uses thereof. In particular, new derivatives of tetrahalogenated benzimidazole with serine/threonine and tyrosine kinases inhibitory properties, preferably selected from the group of PIM, HIPK, DYRK, CLK, CDK, FLT, PKG, Haspin, MER, TAO, MNK, TRK kinases which exhibit superior pharmacological actions, and can be useful for the treatment of disease conditions, especially cancers depending on serine/threonine and tyrosine kinases, such as but not limited to leukemias and solid tumors.Type: ApplicationFiled: December 28, 2011Publication date: July 19, 2012Applicant: SELVITA S.A.Inventors: Krzysztof BRZÓZKA, Wojciech CZARDYBON, Aleksandra SABINIARZ, Mariusz MILLIK, Renata WINDAK, Adrian ZAREBSKI, Nicolas BEUZEN
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Publication number: 20120184556Abstract: Disclosed are substituted benzoimidazolesulfonamides and substituted indolesulfonamides as mGluR4 potentiators.Type: ApplicationFiled: July 23, 2010Publication date: July 19, 2012Inventors: P. Jeffrey Conn, Craig W. Lindsley, Corey R. Hopkins, Charles David Weaver, Colleen M. Niswender, Yiu-Yin Cheung
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Publication number: 20120171129Abstract: Disclosure is provided for benzimidazole derivative compounds that prevent, remove and/or inhibit the formation of biofilms, compositions including these compounds, devices including these compounds, and methods of using the same.Type: ApplicationFiled: June 10, 2010Publication date: July 5, 2012Inventors: Christian Melander, Steven A. Rogers, Robert W. Huigens, III
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Publication number: 20120149676Abstract: 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, L, M, W, R1, R2, R3, R4, R6, R7, R9, Ra, Rb have meanings given in the description.Type: ApplicationFiled: December 8, 2011Publication date: June 14, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Henning PRIEPKE, Henri DOODS, Alexander HEIM-RIETHER, Raimund KUELZER, Roland PFAU, Klaus RUDOLF, Dirk STENKAMP
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Publication number: 20120135987Abstract: This invention is directed to compounds, which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula I. The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention also provides a method of treating a subject suffering from a drug addiction comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I.Type: ApplicationFiled: February 3, 2012Publication date: May 31, 2012Applicant: H. Lundbeck A/SInventors: Andreas Ritzén, Jan Kehler, Morten Langgård, Jacob Nielsen, John Paul Kilburn, Mohamed M. Farah
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Patent number: 8188095Abstract: The present invention relates to compounds which inhibit bacterial gyrase and/or Topo IV and pharmaceutically acceptable compositions comprising said compounds. These compounds, and compositions thereof, are useful in treating bacterial infection. Accordingly, the present invention also relates to methods for treating bacterial infections in mammals.Type: GrantFiled: October 7, 2008Date of Patent: May 29, 2012Assignee: Vertex Pharmaceuticals IncorporatedInventors: Paul Charifson, David Deininger, Anne-Laure Grillot, Yusheng Liao, Steven Ronkin, Dean Stamos, Emanuele Perola, Tiansheng Wang, Arnaud Le Tiran, Joseph Drumm
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Publication number: 20120121540Abstract: Provided are certain chemical entities, pharmaceutical compositions, and methods of treatment of a member of the flaviviradae family of viruses such as hepacivirus (Hepatitis C or HCV).Type: ApplicationFiled: August 8, 2008Publication date: May 17, 2012Inventors: Franz Ulrich Schmitz, Vincent W.F Tai, Roopa Ral, Christopher Don Roberts, Ali Dehghani Mohammad Abadi, Subramanian Baskaran, Irina Slobodov, Jack Maung, Martin Leon Neitzel
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Publication number: 20120122864Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C.Type: ApplicationFiled: December 2, 2009Publication date: May 17, 2012Applicant: PRESIDIO PHARMACEUTICALS, INC.Inventors: Min Zhong, Leping Li
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Patent number: 8178694Abstract: Heterocyclylaminoalkyl Substituted Benzimidazoles Inhibitors of RSV replication of formula (I): The salts and stereochemically isomeric forms thereof, wherein Q is hydrogen, C1-6alkyl optionally substituted with a heterocycle or Q is C1-6alkyl substituted with both —OR4 and a heterocycle; wherein said heterocycle is oxazolidine, thiazolidine, 1-oxo-thiazolidine, 1,1-dioxothiazolidine, morpholinyl, thiomorpholinyl, 1-oxo-thiomorpholinyl, 1,1-dioxothiomorpholinyl, hexahydrooxazepine, hexahydrothiazepine, 1-oxo-hexahydrothiazepine, 1,1-dioxo-hexahydrothiazepine, pyrrolidine, piperidine, homopiperidine, piperazine; which heterocyle may be substituted with 1-2 substituents; each Alk is C1-6alkanediyl; R1 is Ar or optionally substituted piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl, pyridyl, pyrazinyl, pyridazinyl, pyrimidinyl, furanyl, tetrahydrofuranyl, thienyl, pyrrolyl, thiazolyl, oxazolyl, imidazolyl, isothiazolyl, pyrazolyl, isoxazo lyl, oxadiazolyl, quinolinyl, quinoxalinyl, benzofuranyl, benzothienType: GrantFiled: June 20, 2006Date of Patent: May 15, 2012Assignee: Tibotec Pharmaceuticals Ltd.Inventors: Jean-François Bonfanti, Philippe Muller, Jérôme Michel Claude Fortin, Frédéric Marc Maurice Doublet
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Patent number: 8178693Abstract: Disclosed are compounds of the Formula and pharmaceutically acceptable salts and prodrugs thereof, wherein A, R1, R2, R7, R8, and R9 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals. Also disclosed is a method of using such compounds in the treatment of hyperproliferative diseases in mammals, and pharmaceutical compositions containing such compounds.Type: GrantFiled: June 28, 2010Date of Patent: May 15, 2012Assignee: Array Biopharma Inc.Inventors: Eli M. Wallace, Joseph P. Lyssikatos, Allison L. Marlow, T. Brian Hurley
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Publication number: 20120115855Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C.Type: ApplicationFiled: December 2, 2009Publication date: May 10, 2012Applicant: PRESIDIO PHARMACEUTICALS, INC.Inventors: Leping Li, Min Zhong
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Publication number: 20120115903Abstract: Substituted heteroaromatic carboxamide and urea compounds corresponding to formula (i) processes for the preparation thereof, pharmaceutical compositions containing these compounds and also a method of using these compounds in pharmaceutical compositions for treating or inhibiting pain and other conditions mediated at least in part via the vanilloid receptor 1.Type: ApplicationFiled: November 9, 2011Publication date: May 10, 2012Applicant: Gruenenthal GmbHInventors: Robert Frank, Thomas Christoph, Bernhard Lesch, Jeewoo Lee
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Patent number: 8163935Abstract: There is provided a CRF receptor antagonist comprising a compound of the formula (I): wherein R1 is an optionally substituted hydrocarbyl, an optionally substituted C-linked heterocyclic group, an optionally substituted N-linked heteroaryl group, a cyano or an acyl; R2 is an optionally substituted cyclic hydrocarbyl or an optionally substituted heterocyclic group; X is oxygen, sulfur or —NR3— (wherein R3 is a hydrogen, an optionally substituted hydrocarbyl or an acyl); Y1, Y2 and Y3 are each an optionally substituted carbon or a nitrogen, provided that one or less of Y1, Y2 and Y3 is nitrogen; and Z is a bond, —CO—, oxygen, sulfur, —SO—, —SO2—, —NR4—, —NR4-alk-, —CONR4— or —NR4CO— (wherein alk is an optionally substituted C1-4 alkylene and R4 is a hydrogen, an optionally substituted hydrocarbyl or an acyl); or a salt thereof or a prodrug thereof.Type: GrantFiled: April 26, 2006Date of Patent: April 24, 2012Assignee: Takeda Pharmaceutical Company LimitedInventors: Kazuyoshi Aso, Michiyo Mochizuki, Albert Charles Gyorkos, Christopher Peter Corrette, Suk Young Cho, Scott Alan Pratt, Christopher Stephen Siedem
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Publication number: 20120088752Abstract: Heterocyclic compounds that modulate the hedgehog signaling pathway, pharmaceutical composition thereof and their therapeutic applications.Type: ApplicationFiled: June 9, 2010Publication date: April 12, 2012Applicant: SIENA BIOTECH S.p.A.Inventors: J. Russell Thomas, Gal.la Pericot Mohr, Chiara Caramelli, Giacomo Minetto, Marta Bellini
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Patent number: 8148363Abstract: The present invention relates to novel heterocyclic compounds of Formulae I-III; as disclosed herein or a pharmaceutically acceptable salt, solvate, ester, prodrug or stereoisomer thereof. Also disclosed are pharmaceutical compositions comprising said compounds, and methods for using said compounds for treating or preventing a thromboembolic disorder.Type: GrantFiled: May 18, 2009Date of Patent: April 3, 2012Assignee: Schering CorporationInventors: Martin C. Clasby, William J. Greenlee, Yan Xia, Tin-Yau Chan, Mariappan V. Chelliah, Samuel Chackalamannil, Haiyan Pu, Keith A. Eagen, Henry Vaccaro, Brian A. McKittrick, Liyuan Wang, Xiaobang Gao
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Publication number: 20120076756Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: October 4, 2011Publication date: March 29, 2012Inventors: Yao-Ling Qiu, Ce Wang, Xiaowen Peng, Lu Ying, Yat Sun Or
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Patent number: 8143282Abstract: The present invention relates to compounds which are inhibitors of histone deacetylase. More particularly, the present invention relates to heterocyclic compounds and methods for their preparation. These compounds may be useful as medicaments for the treatment of proliferative disorders as well as other diseases involving, relating to or associated with enzymes having histone deacetylase (HDAC) activities.Type: GrantFiled: August 1, 2006Date of Patent: March 27, 2012Assignee: S*BIO Pte Ltd.Inventors: Dizhong Chen, Weiping Deng, Ken C. Lee, Pek L. Lye, Eric T. Sun, Haishan Wang, Niefang Yu
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Patent number: 8138168Abstract: The invention relates to compounds having the formulae: wherein the variables are as defined herein. The invention further relates to methods of making and using these compounds, and pharmaceutical compositions, kits and articles of manufacture comprise the compounds.Type: GrantFiled: September 26, 2008Date of Patent: March 20, 2012Assignee: Takeda Pharmaceutical Company LimitedInventors: Benjamin Jones, Stephen W. Kaldor, Walter Keung, Andre A. Kiryanov, Zhe Li, Jeffrey A. Stafford, John Tyhonas, Craig Behnke
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Publication number: 20120058085Abstract: This invention relates to derivatives of 1-(p-chlorobenzyl)-2-(1-pyrrolidinylmethyl)benzimidazole according to Formula I wherein at least one Y is deuterium described herein and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering an inhibitor of hepatitis C virus (HCV) RNA replication.Type: ApplicationFiled: May 14, 2010Publication date: March 8, 2012Inventors: Rose A. Persichetti, Julie F. Liu, Adam Morgan
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Publication number: 20120046303Abstract: Compounds which inhibit the activity of poly(ADP-ribose)polymerase (PARP), compositions containing the compounds and methods of treating diseases using them are disclosed.Type: ApplicationFiled: October 27, 2011Publication date: February 23, 2012Applicant: ABBOTT LABORATORIESInventors: Virajkumar B. Gandhi, Vincent L. Giranda, Jianchun Gong, Thomas D. Penning, Gui-Dong Zhu
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Publication number: 20120040977Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C.Type: ApplicationFiled: February 22, 2010Publication date: February 16, 2012Applicant: PRESIDIO PHARMACEUTICALS, INC.Inventors: Leping Li, Min Zhong
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Publication number: 20120040960Abstract: The present invention comprises compounds of Formula (I): wherein: X, R1, R2, R3, and R4 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: ApplicationFiled: October 25, 2011Publication date: February 16, 2012Inventors: Xuqing Zhang, Heather Rae Hufnagel, Cuifen Hou, Dana L. Johnson, Zhihua Sui
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Publication number: 20120022090Abstract: The present invention is concerned with novel substituted benzoxazole, benzimidazole, oxazolopyridine and imidazopyridine derivatives of Formula (I) wherein R1, R2, R3, R4, X, A1, A2, A3, A4, Y1, Y2, Y3 and Z have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.Type: ApplicationFiled: February 15, 2010Publication date: January 26, 2012Inventors: Henricu Jacobus Maria Gijsen, Francois Paul Bischoff, Wei Zhuang, Sven Franciscus Anna Van Brandt, Michel Surkyn, Mirko Zaja, Didier Jean-Claude Berthelot, Michel Anna Jozef Cleyn, Gregor James Macdonald, Daniel Oehlrich
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Patent number: 8101643Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: GrantFiled: March 1, 2010Date of Patent: January 24, 2012Assignee: Enanta Pharmaceuticals, Inc.Inventors: Yao-Ling Qiu, Ce Wang, Xiaowen Peng, Lu Ying, Yat Sun Or
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Publication number: 20120016449Abstract: Methods and devices related to the treatment of diseases using phototherapy are described. Some embodiments provide an organic light-emitting diode device, such as a light-emitting device for phototherapy, comprising a compound of Formula 1. Methods of treating disease diseases with phototherapy are also described.Type: ApplicationFiled: July 15, 2011Publication date: January 19, 2012Applicant: Nitto Denko CorporationInventors: Amane Mochizuki, Sazzadur Rahman Khan, Shijun Zheng, Keisaku Okada
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Publication number: 20120007063Abstract: The present invention relates to the use of dibenzofurans and dibenzothiophenes which have at least one nitrogen-bonded five-membered heterocyclic ring as a substituent as host, blocker and/or charge transport material in organic electronics. The present invention further relates to dibenzofurans and dibenzothiophenes which comprise at least one nitrogen-bonded five-membered heterocyclic ring and at least one carbazolyl radical as substituents, to a process for preparation thereof, and to the use of these compounds in organic electronics.Type: ApplicationFiled: July 8, 2011Publication date: January 12, 2012Applicant: BASF SEInventors: Nicolle LANGER, Christian Schildknecht, Christian Lennartz, Gerhard Wagenblast, Thomas Schäfer
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Patent number: 8093275Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, X, Y, R1, R2, R3, R4, R5, R6 and R7 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: January 10, 2012Assignee: Roche Palo Alto LLCInventors: Li Chen, Michael Patrick Dillon, Lichun Feng, Minmin Yang
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Patent number: 8088767Abstract: This invention relates to the field of protein tyrosine kinases and inhibitors thereof. In particular, the invention relates to inhibitors of JAK-2, pharmaceutical compositions of the compounds for inhibiting JAK-2, methods of inhibiting JAK-2 in a cell, comprising contacting a cell in which inhibition of JAK-2 is desired with a compound or pharmaceutical composition comprising a compound according to the invention. The also comprises methods of treating a disease or condition that involves JAK-2 comprising administering to a patient a pharmaceutical composition comprising a compound according to the invention.Type: GrantFiled: September 28, 2007Date of Patent: January 3, 2012Assignee: Exelixis, Inc.Inventors: Adam Antoni Galan, Jeff Chen, Hongwang Du, Timothy Forsyth, Tai Phat Huynh, Henry William Beecroft Johnson, Patrick Kearney, James W. Leahy, Matthew Sangyup Lee, Grace Mann, Brian Hugh Ridgway, Craig Stacy Takeuchi, Peiwen Zhou