Plural Piperidine Rings Patents (Class 514/316)
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Publication number: 20120238602Abstract: The present invention relates to piperidine sulphonamide derivatives of formula wherein Ar1, Ar2, R1, R2, m and n are as defined in the description and claims, or pharmaceutically suitable acid addition salts thereof. The compounds of formula I are orexin receptor antagonists and the related compounds can be useful in the treatment of sleep apnea, narcolepsy, insomnia, parasomnia, jet lag syndrome, circadian rhythms disorder or sleep disorders associated with neurological diseases.Type: ApplicationFiled: May 23, 2012Publication date: September 20, 2012Inventors: Henner Knust, Matthias Nettekoven, Emmanuel Pinard, Olivier Roche, Mark Rogers-Evans
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Publication number: 20120238574Abstract: The present invention relates to (1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl derivatives having the general formula (I) to pharmaceutical compositions comprising the same and to the use of these (1,1,1,3,3,3-hexafluoro-2-hydroxy-propan-2-yl)phenyl derivatives in the treatment of atherosclerosis.Type: ApplicationFiled: October 26, 2010Publication date: September 20, 2012Applicant: N.V. ORGANONInventors: Andrew John Cooke, Emma Louise Carswell, David Jonathan Bennett
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Publication number: 20120225889Abstract: The present invention provides use of the compounds represented by formula (1): wherein, R1, R2, R3 and R4 are as defined in the specification, in all their stereo isomeric and tautomeric forms and mixtures thereof in all ratios, and their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, pharmaceutically acceptable polymorphs and prodrugs and pharmaceutical compositions containing them for treatment of inflammatory disorders mediated by one or more cytokines selected from Tumor Necrosis Factor-alpha (TNF-?), interferon-? (IFN-?) and interleukins such as IL-1?, IL-2, IL-6, and IL-8. The present invention also relates to a pharmaceutical composition adapted for use in the treatment of inflammatory disorders. The present invention further provides a method of treatment of inflammatory disorders by administering a therapeutically effective amount of the said compound of formula (1) or its pharmaceutical composition, to a mammal in need thereof.Type: ApplicationFiled: November 15, 2010Publication date: September 6, 2012Applicant: PIRAMAL LIFE SCIENCES LIMITEDInventors: Asha Kulkarni-Almeida, Ravindra Dattatraya Gupte, Nilesh Madhukar Dagia, Prabha Beerchandra Mishra
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Publication number: 20120225868Abstract: The present invention is concerned with novel dual modulators of the 5-HT2A and D3 receptors of formula (I) wherein n, Y, R1, R2, R3, and R4 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions containing them and their use as pharmaceuticals.Type: ApplicationFiled: February 27, 2012Publication date: September 6, 2012Inventors: Rosa Maria Rodriguez Sarmiento, Juergen Wichmann
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Patent number: 8258156Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of GPR119.Type: GrantFiled: May 23, 2011Date of Patent: September 4, 2012Assignee: IRM LLCInventors: Phillip B. Alper, Mihai Azimioara, Christopher N. Cow, Robert Epple, Pierre-Yves Michellys, Victor Nikulin
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Publication number: 20120220564Abstract: Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted T-type calcium channel activity are disclosed using a series of compounds containing N-acylated cyclic amines linked to an a?l ring as shown in formula (I).Type: ApplicationFiled: September 17, 2010Publication date: August 30, 2012Applicant: Zalicus Pharmaceuticals Ltd.Inventors: Hassan Pajouhesh, Yongbao Zhu, Yuanxi Zhou, Michael E. Grimwood, Eric Simonson
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Publication number: 20120220563Abstract: The invention relates to novel substituted piperidines, to processes for preparation thereof, to the use thereof for treatment and/or prophylaxis of diseases and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially of cardiovascular disorders and tumour disorders.Type: ApplicationFiled: May 19, 2010Publication date: August 30, 2012Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Dirk Heimbach, Susanne Röhrig, Yolanda Cancho Grande, Eckhard Bender, Katja Zimmermann, Anja Buchmüller, Christoph Gerdes, Mark Jean Gnoth, Kersten Matthias Gericke, Mario Jeske
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Publication number: 20120220562Abstract: Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.Type: ApplicationFiled: February 24, 2012Publication date: August 30, 2012Applicant: ABBOTT LABAORATORIESInventors: David A DeGoey, Warren M. Kati, Charles W. Hutchins, Pamela L. Donner, Allan C. Krueger, John T. Randolph, Sachin V. Patel, Mark A. Matulenko, Ryan G. Keddy, Tammie K. Jinkerson, Yi Gao, Dachun Liu, John K. Pratt, Todd W. Rockway, Clarence J. Maring, Douglas K. Hutchinson, Charles A. Flentge, Rolf Wagner, David A. Betebenner, Kathy Sarris, Kevin R. Woller, William A. Carroll
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Patent number: 8252800Abstract: The present invention relates to compounds of the Formula I, the pharmaceutically acceptable salts and stereoisomers thereof, which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions in mammals: wherein n is an integer, preferably n is 1; wherein R1 and R2 are independently selected from the group consisting of:Type: GrantFiled: July 28, 2009Date of Patent: August 28, 2012Inventors: Wayne R. Danter, Martyn Brown, George Ma, Ghenadie Rusu, Jianhua Zhong, Natalie Lazarowych, Stephen Houldsworth
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Publication number: 20120214788Abstract: The invention relates to novel heteroaryl-substituted piperidines, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular of cardiovascular diseases and tumour diseases.Type: ApplicationFiled: February 20, 2012Publication date: August 23, 2012Applicant: Bayer Pharma AktiengesellschaftInventors: Dirk Heimbach, Susanne Röhrig, Dirk Schneider, Ulrich Rester, Eckhard Bender, Mark Meininghaus, Katja Zimmermann, Dmitry Zubov, Anja Buchmüller, Georges Von Degenfeld, Christoph Gerdes, Michael Gerisch, Mark Jean Gnoth, Yolanda Cancho Grande, Mario Jeske, Kersten Matthias Gericke
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Publication number: 20120214790Abstract: The present invention provides compounds which show high effectiveness against positive symptoms, negative symptoms and cognitive dysfunction in schizophrenia and reduce conventional side-effect risks as well as have remarkable effects for central neurological diseases associated with cognitive dysfunction other than schizophrenia. N-Acyl cyclic amine derivatives of formula (1): wherein Ar1 and Ar2 are aryl or heteroaryl; V is nitrogen, or CR3; W1 is a single bond, —C(O)—, etc.; W2 is C1-alkylene; W3 is a single bond, methylene, —NH—, —CR4?CR5—, etc.; Ring Q is a group of formula (a) in which n is 0 or 1; m is 0 to 2; k is 1 to 3; Z is a single bond, methylene, oxygen, etc.; R1a, R1b and R1c are each, same or different, hydrogen, hydroxyl, halogen, cyano, C1-6 alkyl, etc.; or pharmaceutically acceptable salts thereof are provided.Type: ApplicationFiled: March 11, 2011Publication date: August 23, 2012Inventors: Megumi Maruyama, Naoya Kinomura, Satoshi Nojima, Masahiro Takamura, Keisuke Kakiguchi, Hiroto Tatamidani
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Publication number: 20120214798Abstract: The present invention relates to novel hepcidin antagonists of formula (I), pharmaceutical compositions comprising them and the use thereof as medicaments, in particular for treatment of disorders in iron metabolism, such as, in particular, iron deficiency diseases and anaemias, in particular anaemias in connection with chronic inflammatory diseases (ACD: anaemia of chronic disease and AI: anaemia of inflammation).Type: ApplicationFiled: September 6, 2010Publication date: August 23, 2012Applicant: VIFOR (INTERNATIONAL) AGInventors: Franz Dürrenberger, Susanna Burckhardt, Wilm Buhr, Peter O. Geisser, Felix Funk, Vincent A. Corden, Stephen M. Courtney, Tara Davenport, Stefan Jaeger, Mark P. Ridgill, Mark Slack, Christopher J. Yarnold, Wei Tsung Yau
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Publication number: 20120208844Abstract: The present invention provides a compound of Formula (1) as described herein or a pharmaceutically acceptable salt, solvate or ester thereof. The compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and methods of treating cancer using the same.Type: ApplicationFiled: October 5, 2010Publication date: August 16, 2012Inventors: Stephane L. Bogen, Yao Ma, Yaolin Wang, Brian Robert Lahue, Latha G. Nair, Manami Shizuka, Matthew Ernst Voss, Margarita Kirova-Snover, Weidong Pan, Yuan Tian, Bheemashankar A. Kulkarni, Craig R. Gibeau, Yuan Liu, Giovanna Scapin, Diane Rindgen, Ronald J. Doll, Timothy J. Guzi, Danny J. Hicklin, Amin Nomeir, Cynthia Seidel-Dugan, Gerald W. Shipps, JR., Malcolm MacCoss
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Patent number: 8242137Abstract: The invention provides crystalline forms of biphenyl-2-ylcarbamic acid 1-(2-{[4-(4-carbamoylpiperidin-1-ylmethyl)benzoyl]methylamino}ethyl)piperidin-4-yl ester, and pharmaceutically acceptable solvates thereof. The crystalline form can be a freebase, or a salt such as a diphosphate, monosulfate or dioxalate salt. The invention also provides pharmaceutical compositions comprising these crystalline compounds or prepared using these compounds; processes and intermediates for preparing the crystalline compounds; and methods of using these compounds to treat a pulmonary disorder.Type: GrantFiled: September 21, 2009Date of Patent: August 14, 2012Assignee: Theravance, Inc.Inventors: Sabine Axt, Timothy J. Church
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Publication number: 20120202775Abstract: Compounds having drug and bio-affecting properties are described herein, including their properties, pharmaceutical compositions and methods of use. In particular, tricyclic aryl or heteroaryl piperazine diamide derivatives that possess unique antiviral activity are set forth. These compounds are useful for the treatment of HIV and AIDS.Type: ApplicationFiled: August 4, 2011Publication date: August 9, 2012Inventors: Tao Wang, Zhongxing Zhang, Zhiwei Yin, John F. Kadow, Nicholas A. Meanwell
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Publication number: 20120202795Abstract: The present invention relates to a series of 2,3,5-substituted pyridone derivatives of formula I: wherein R, R1, R2, R3 and R4 are as defined herein. This invention also relates to methods of making these compounds. The compounds of this invention are inhibitors of poly(adenosine 5?-diphosphate ribose) polymerase (PARP) and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases, including diseases associated with the central nervous system and cardiovascular disorders.Type: ApplicationFiled: April 18, 2012Publication date: August 9, 2012Applicant: AVENTIS PHARMACEUTICALS INC.Inventors: Philip M. WEINTRAUB, Paul R. EASTWOOD, Shujaath MEHDI, David W. STEFANY, Kwon Yon MUSICK, Neil MOORCROFT, Sungtaek LIM, John Z. JIANG, Hartmut RUTTEN, Stefan PEUKERT, Uwe SCHWAHN
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Publication number: 20120190657Abstract: This invention provides compounds of formula I: wherein a, b, c, d, m, n, p, s, t, W, Ar1, R1, R2, R3, R4, R6, R7, and R8 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.Type: ApplicationFiled: April 3, 2012Publication date: July 26, 2012Applicant: THERAVANCE, INC.Inventors: Mathai Mammen, Yu-Hua Ji, YongQi Mu, Craig Husfeld, Li Li
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Patent number: 8222255Abstract: Novel derivatives of enfumafungin are disclosed herein, along with their, pharmaceutically acceptable salts, hydrates and prodrugs. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and methods of using such compounds as antifungal agents and/or inhibitors of (1,3)-?-D-glucan synthase. The disclosed compounds, their pharmaceutically acceptable salts, hydrates and prodrugs, as well as compositions comprising such compounds, salts, hydrates and prodrugs, are useful for treating and/or preventing fungal infections and associated diseases and conditions.Type: GrantFiled: September 25, 2008Date of Patent: July 17, 2012Assignees: Merck Sharp & Dohme Corp., Scynexis, Inc.Inventors: James M. Balkovec, Phieng Siliphaivanh, Frances A. Bouffard, Roland A. Bouffard, legal representative, Michael R. Peel, Weiming Fan, Ahmed Mamai, Sarah Dimick Gray
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Publication number: 20120178681Abstract: Bipiperidinyl compounds of the formula I, are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts and solvates are included as well. The compounds are useful as agonists of the g-protein coupled receptor GPR-119.Type: ApplicationFiled: March 21, 2012Publication date: July 12, 2012Applicant: Merck Sharp & Dohme Corp.Inventors: HAROLD B. WOOD, Alan D. Adams, Stanley Freeman, Jason W. Szewczyk, Conrad Santini, Yong Huang
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Publication number: 20120172358Abstract: Compounds of formula (I): or pharmaceutically acceptable salts thereof, are GPCR agonists and are useful as for the treatment of obesity and diabetes.Type: ApplicationFiled: February 14, 2012Publication date: July 5, 2012Applicant: Prosidion LimitedInventors: Stuart Edward Bradley, Matthew Colin Thor Fyfe, Lisa Sarah Bertram, William Gattrell, Revathy Perpetua Jeevaratnam, John Keily, Martin James Procter, Chrystelle Marie Rasamison, Philip John Rushworth, Colin Peter Sambrook-Smith, David French Stonehouse, Simon Andrew Swain, Geoffrey Martyn Williams
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Patent number: 8207344Abstract: GPR119 agonist compounds of the formula: and pharmaceutical compositions for the treatment of diabetes and obesity.Type: GrantFiled: July 12, 2010Date of Patent: June 26, 2012Assignee: Eli Lilly and CompanyInventors: David Gene Barrett, Ana Belen Bueno Melendo, Jeffry Bernard Franciskovich, Bin Liu, Kumiko Takeuchi
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Publication number: 20120157449Abstract: The present invention is concerned with novel dual modulators of the 5-HT2A and D3 receptors of formula (I) wherein n, x, Y, R1, R2, R3, and R4 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as pharmaceuticals.Type: ApplicationFiled: December 7, 2011Publication date: June 21, 2012Inventors: Rosa Maria Rodriguez Sarmiento, Juergen Wichmann
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Publication number: 20120149731Abstract: The present invention relates to a method of treatment of urticaria comprising administration to a patient in need thereof an amount of the compound 3-(4-{[4-(4-{[3-(3,3-dimethyl-1-piperidinyl) propyl]oxy}phenyl)-1-piperidinyl]carbonyl}-1-naphthalenyl)propanoic acid, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: June 24, 2010Publication date: June 14, 2012Applicant: GLAXO GROUP LIMITEDInventors: Kenneth Lyle Clark, Edward Earl Philpot
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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: 20120141491Abstract: The subject application provides small compounds that are able to increase/enhance autophagy in various cells. These compounds are useful in augmenting existing treatments of various cancers, microbial/viral infections, and neurodegenerative diseases. Thus, the subject application also provides methods of treating various types of cancers, microbial/viral infections, and neurodegenerative diseases.Type: ApplicationFiled: August 9, 2010Publication date: June 7, 2012Applicant: University of Florida Research Foundation Inc.Inventors: William A. Dunn, Debra Everton Akin, Brian Keith Law
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Publication number: 20120136027Abstract: Inhibitors of HCV replication of formula I including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein R and R* have the meaning defined in the claims. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HCV inhibitors, in the treatment or prophylaxis of HCV.Type: ApplicationFiled: August 6, 2010Publication date: May 31, 2012Inventors: David Mc Gowan, Samuel Dominique Demin, Stefaan Julien Last, Koen Vandyck, Pierre Jean-Marie Bernard Raboisson
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Patent number: 8188288Abstract: The present invention relates to 2-adamantylurea derivatives of formula I as selective inhibitors of the enzyme 11-beta-hydroxysteroid dehydrogenase type 1 (11?-HSD1) and the use of such compounds for the treatment and prevention of metabolic syndrome, diabetes, insulin resistance, obesity, lipid disorders, glaucoma, osteoporosis, cognitive disorders, anxiety, depression, immune disorders, hypertension and other diseases and conditions.Type: GrantFiled: November 22, 2006Date of Patent: May 29, 2012Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Denis Carniato, Christine Charon, Johannes Gleitz, Didier Roche, Bjoern Hock
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Patent number: 8188287Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5 and X are as defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is uveitis, including acute, recurring or chronic uveitis. 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 19, 2009Date of Patent: May 29, 2012Assignee: Janssen Pharmaceutica N.V.Inventors: Chaozhong Cai, Zhihua Sui
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Publication number: 20120129827Abstract: The present invention relates to novel derivatives of 1-alkyl-6-oxo-piperidine-3-carboxylic acids and 1-alkyl-5-oxo-pyrrolidine-3-carboxylic acids represented by Formula I: wherein n is an integer of 1 or 2; R1, R2, R3, and R4 are each independently selected from the group consisting of hydrogen and methyl; X is selected from the group consisting of oxygen and nitrogen; and R5 is hydrogen or a C1-C7 linear or branched acyclic hydrocarbon group, or R5 together with X form a 3- to 8-membered heterocyclic hydrocarbon group, and their uses as cooling compounds.Type: ApplicationFiled: November 22, 2010Publication date: May 24, 2012Inventor: Arkadiusz Kazimierski
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Publication number: 20120130147Abstract: Compounds of the formula (I), in which R1, R2, R3, R4, and q have the meanings indicated in Claim 1, can be employed, inter alia, for the treatment of tumours.Type: ApplicationFiled: January 25, 2012Publication date: May 24, 2012Inventors: Dirk FINSINGER, David Bruge, Hans-Peter Buchstaller, Ulrich Emde, Kai Schiemann, Wolfgang Staehle, Christiane Amendt, Nina Heiss, Frank Zenke
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Publication number: 20120129831Abstract: The invention relates to novel substituted piperidines, to processes for preparation thereof, to the use thereof for treatment and/or prophylaxis of diseases and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially of cardiovascular disorders and tumour disorders.Type: ApplicationFiled: May 14, 2010Publication date: May 24, 2012Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Dirk Heimbach, Susanne Röhrig, Yolanda Cancho Grande, Dirk Schneider, Ulrich Rester, Eckhard Bender, Mark Meininghaus, Katja Zimmermann, Dmitry Zubov, Anja Buchmüller, Georges Von Degenfeld, Christoph Gerdes, Michael Gerisch, Mark Jean Gnoth, Kersten Matthias Gericke, Mario Jeske
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Publication number: 20120129837Abstract: Chemical agents, such as disulfonamide derivatives of fluorene, anthracene, xanthene, dibenzosuberone and acridine, and similar heterocyclic ring structures, including salts thereof, that act as anti-cancer and anti-tumor agents, especially where such agents modulate the activity of the Wnt/?-catenin signaling pathway, and serve to reduce ?-catenin levels present in cells, such as cancer cells, or where the agents modulate levels of gene expression in cellular systems, including cancer cells, are disclosed, along with methods for preparing such agents, as well as pharmaceutical compositions containing such agents as active ingredients and methods of using these as therapeutic agents.Type: ApplicationFiled: January 30, 2012Publication date: May 24, 2012Inventors: Wieslaw M. Cholody, Yi Zang, Norman E. Ohler, Sheela Chellappan, Janak Padia, Karina Zuck, Jeffrey W.H. Watthey, Zoe Ohler, Jeffrey Strovel
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Patent number: 8178531Abstract: The present invention relates to antiviral compounds of formula (I), compositions containing these compounds, processes for their preparation, intermediates in their synthesis, and their use as therapeutics for prevention of organ transplantation rejection, the treatment of immune disorders and inflammation, and treatment of viral (particularly hepatitis C viral) infection.Type: GrantFiled: February 23, 2011Date of Patent: May 15, 2012Assignee: Enanta Pharmaceuticals, Inc.Inventors: Yat Sun Or, Guoqiang Wang, Xuri Gao
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Publication number: 20120115906Abstract: The invention relates to compounds of the formula (I), where: R1 is: a —NR5R6 group; an unsubstituted or substituted phenyl; R2 is: a (C1-C4)alkyl; an —X—R7 group; R3 and R4 each are independently a substituted phenyl; R5 is a hydrogen atom or a (C1-C4)alkyl; R6 is an unsubstituted or substituted (C1-C4)alkyl; or R5 and R6 together with the nitrogen atom to which they are bonded constitute an unsubstituted or substituted heterocyclic compound; X is a (C1-C5)alkylene; R7 is an —OR8 group, a —NR9R10 group, an —SO2—(C1-C4)alkyl group; R8 is a hydrogen atom or a (C1-C4)alkyl; R9 is a hydrogen atom or a (C1-C4)alkyl; R10 is a hydrogen atom, a —COR11 group, an —SO2R11 group or a —CO(CH2)mOH group; R11 is an unsubstituted or substituted (C1-C4)alkyl; m is 1, 2 or 3. The invention also relates to methods for preparing same and to the therapeutic use thereof.Type: ApplicationFiled: March 25, 2010Publication date: May 10, 2012Applicant: SANOFIInventors: Jean-Philippe Ducoux, Murielle Rinaldi-Carmona, Arnaud Rouquette
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Publication number: 20120115838Abstract: Disclosed are carboxamide, sulfonamide and amine compounds, as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure in which R1, R2, R4, E, T, n and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.Type: ApplicationFiled: January 11, 2012Publication date: May 10, 2012Applicant: RIGEL PHARMACEUTICALS, INC.Inventors: Hui Hong, Xiang Xu, Jiaxin Yu, Rajinder Singh, Ihab S. Darwish, Sambaiah Thota
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Publication number: 20120115907Abstract: The present invention relates to novel renin inhibitors of general formula (1), novel intermediates involved in their synthesis, their pharmaceutically acceptable salts and pharmaceutical compositions containing them. The present invention also relates to a process of preparing compounds of general formula (1), their tautomeric forms, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and novel intermediates involved in their synthesis.Type: ApplicationFiled: April 22, 2010Publication date: May 10, 2012Applicant: CADILA HEALTHCARE LIMITEDInventors: Pravain Thombare, Jigar Desai, Mukul R. Jain
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Publication number: 20120108606Abstract: Disclosed are carboxamide, sulfonamide and amine compounds, as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure in which R1, R2, R4, D, E, J, T, p, q and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.Type: ApplicationFiled: January 11, 2012Publication date: May 3, 2012Applicant: RIGEL PHARMACEUTICALS, INC.Inventors: Ihab S. Darwish, Jiaxin Yu, Hui Hong, Rajinder Singh, Sambaiah Thota, Xiang Xu
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Patent number: 8158651Abstract: The treatment of acute pain with a sufficient dosage by intranasal administration of fentanyl results in a time to onset of action comparable to intravenous administration and a significantly faster onset of action than nasal titration of fentanyl. The nasal administration of a sufficient amount of fentanyl to obtain pain relief has lower maximum plasma concentrations comparable to intravenous administration and results in lower rates of adverse events like respiratory depression, nausea and vomiting. Compositions fur use in the method are also disclosed.Type: GrantFiled: January 24, 2007Date of Patent: April 17, 2012Assignee: Nycomed Danmark ApsInventors: Jesper Grarup, Hanne Wulf Nielsen
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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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Publication number: 20120088791Abstract: In one aspect, the invention relates to compounds having a general structure: Formula (I) which are useful as allosteric agonists of the M1 muscarinic receptor, synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurodegenerative diseases, including Alzheimer's Disease. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: February 19, 2010Publication date: April 12, 2012Applicant: VANDERBILT UNIVERSITYInventors: Craig W. Lindsley, Jeffrey P. Corn, Charles David Weaver, Colleen M. Niswender, Evan P. Lebois, Thomas M. Bridges
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Patent number: 8153657Abstract: One aspect of the invention relates to piperidine compounds that are useful as inhibitors of monoamine transporters. The invention also relates to pharmaceutical compositions, comprising a piperidine compound of the invention. Another aspect of the present invention relates to the use of the aforementioned compounds in a method of treating a disorder of the central nervous system in a mammal.Type: GrantFiled: October 22, 2004Date of Patent: April 10, 2012Assignee: Georgetown UniversityInventors: Alan P. Kozikowski, Jia Zhou
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Publication number: 20120083499Abstract: The present application relates to calcium channel inhibitors comprising compounds of formula (I), formula (II), formula (III), or formula (IV), wherein L1, R1, R2, R3, R4, R5, R6, R7 and Rc are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.Type: ApplicationFiled: December 12, 2011Publication date: April 5, 2012Applicant: ABBOTT LABORATORIESInventors: Qingwei Zhang, Andrew O. Stewart, Zhiren Xia
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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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Publication number: 20120077794Abstract: The invention provides novel bis-pyridylpyridones which are antagonists at the melanin-concentrating hormone receptor 1 (MCHR1), pharmaceutical compositions containing them, processes for their preparation, and their use in therapy and for the treatment of obesity and diabetes.Type: ApplicationFiled: June 2, 2010Publication date: March 29, 2012Applicant: GLAXSMITHKLINE LLCInventors: Siegfried Benjamin Christensen, IV, Donghui Qin, Shenglin Chen, Xing Huang, Di Li, Fei Li, Xiaojuan Lin, Shi Lu, Maoyun Lv, Chengde Wu, Weiliang Xu, Gang Yan, Jianxing Yuan, Weina Zhang, Zhiliu Zhang
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Patent number: 8143279Abstract: The invention relates to benzimidazole-carboxamide 5-HT4 receptor agonist compounds of formula (I) wherein R1 and X are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The invention also relates to pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds. The invention further relates to crystalline forms of a compound of formula (I).Type: GrantFiled: May 24, 2006Date of Patent: March 27, 2012Assignee: Theravance, Inc.Inventors: Robert Murray McKinnell, Daniel D. Long, Sean Dalziel, Kirsten M. Phizackerley
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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: 20120065230Abstract: Nitroxide free radicals attached to antineoplastic agents can synergize their potencies to cancer cells. This invention relates to any antineoplastic agents and their derivatives chemically attached with nitroxide free radicals, such as TEMPO and its radical derivatives. This invention also relates to precursors of such compounds, as well as the products formed from the adducts after administration.Type: ApplicationFiled: March 21, 2011Publication date: March 15, 2012Applicant: The Trustees of California State UniversityInventors: Yong Ba, Errol V. Mathias
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Publication number: 20120059014Abstract: The present invention is directed to therapeutic compounds of the following formula (I) which have activity as agonists of GPR119 and are useful for the treatment of metabolic disorders including type II diabetes.Type: ApplicationFiled: March 12, 2010Publication date: March 8, 2012Applicant: PROSIDION LIMITEDInventors: Oscar Barba, Tom Banksia Dupree, Peter Timothy Fry, Matthew Colin Thor Fyfe, Revathy Perpetua Jeevaratnam, Thomas Martin Krulle, Karen Lesley Schofield, Donald Smyth, Thomas Staroske, Alan John William Stewart, David French Stonehouse, Simon Andrew Swain, David Matthew Withall
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Patent number: 8124624Abstract: Substituted sulfonamide compounds corresponding to formula I: a process for their preparation, pharmaceutical compositions comprising such compounds, and the use of such substituted sulfonamide compounds in pharmaceutical compositions for the treatment of pain or other disorders or diseases that are mediated at least in part by B1R receptors.Type: GrantFiled: April 8, 2009Date of Patent: February 28, 2012Assignee: Gruenenthal GmbHInventors: Stefan Oberboersch, Melanie Reich, Stefan Schunk, Michael Engels, Ruth Jostock, Tieno Germann, Sabine Hees
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Publication number: 20120046276Abstract: A method of preventing or treating diseases caused by Mycobacterium, comprising administering to a subject in need of such treatment an effective amount of a pleuromutilin.Type: ApplicationFiled: October 25, 2011Publication date: February 23, 2012Applicant: Nabriva Therapeutics AGInventors: Gerd Ascher, Heinz Berner, Rosemarie Mang