The Ring Nitrogens Are Bonded Directly To Each Other (e.g., Pyridazine, Etc.) Patents (Class 514/236.5)
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Patent number: 8853205Abstract: Disclosed are biologically active hetero pyrrole analogs such as imidazoles, thiazoles, oxazoles and pyrazoles capable of interacting with the CB1 and/or CB2 cannabinoid receptors. Aspects disclose hetero pyrrole analogs acting as CB1 and/or CB 1 receptor antagonists, having selectivity for the CB 1 or CB2 receptor, acting as neutral antagonists, acting preferentially on CB 1 receptors located in the peripheral nervous system, and/or acting as nitric oxide donors. Pharmaceutical preparations employing the disclosed analogs and methods of administering therapeutically effective amounts of the disclosed analogs to provide a physiological effect are also disclosed.Type: GrantFiled: February 19, 2009Date of Patent: October 7, 2014Assignee: University of ConnecticutInventors: Alexandros Makriyannis, Venkata Kiran Vemuri
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Publication number: 20140296200Abstract: The present invention provides compounds of the formula: which are useful as inhibitors of PHD, pharmaceutical compositions thereof, methods for treatment of conditions associated with HIF, processes for making the compounds and intermediates thereof.Type: ApplicationFiled: March 26, 2014Publication date: October 2, 2014Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Jason W. Brown, Melinda Davis, Anthony Ivetac, Benjamin Jones, Andre A. Kiryanov, Jon Kuehler, Marion Lanier, Joanne Miura, Sean Murphy, Xiaolun Wang
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Publication number: 20140296238Abstract: Novel dihydropyrazole derivatives of formula (I) wherein L, R, R3, R4, R5, R6, R7, X1, X2, X3, X4, Y, m and n have the meaning according to the claims, are positive allosteric modulators of the FSH receptor, and can be employed, inter alia, for the treatment of fertility disorders.Type: ApplicationFiled: June 10, 2014Publication date: October 2, 2014Inventors: Henry YU, Thomas E. RICHARDSON, Robert James FOGLESONG, Lizbeth Celeste DESELM, Andreas GOUTOPOULOS
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Publication number: 20140288041Abstract: The present invention relates to aryl- or heteroaryl-substituted benzene compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.Type: ApplicationFiled: May 12, 2014Publication date: September 25, 2014Applicant: EPIZYME, INC.Inventors: Kevin Wayne Kuntz, Richard Chesworth, Kenneth William Duncan, Heike Keilhack, Natalie Warholic, Christine Klaus, Sarah Kathleen Knutson, Timothy James Nelson Wigle, Masashi Seki, Syuji Shirotori, Satoshi Kawano
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Publication number: 20140288044Abstract: The invention relates to compounds, pharmaceutical compositions and medicaments comprising such compounds, and the use of these compounds, compositions, and medicaments in methods of treating diseases and disorders.Type: ApplicationFiled: April 12, 2012Publication date: September 25, 2014Applicant: Alzheimer's Institute of America, Inc.Inventors: Ryan Holcomb, Paul R. Sebahar, Kazuyuki Suzuki, Donald A. McLeod, David M. Dastrup, Christophe Hoarau, Robert J. Halter, Matthew Gregory Bursavich, Mark D. Shenderovich, Burt Richards, Paul L. Bartel
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Publication number: 20140288074Abstract: Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, fungicides: wherein Q1, R1, R1a, R2, R3 and X are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.Type: ApplicationFiled: March 21, 2014Publication date: September 25, 2014Applicant: E I DU PONT DE NEMOURS AND COMPANYInventors: ANDREW EDMUND TAGGI, Jeffrey Keith Long, Moumita Kar
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Publication number: 20140275049Abstract: The present invention provides compounds of Formula I or a pharmaceutical salt thereof; methods of treating osteoarthritis and the pain associated with osteoarthritis using the compounds; and processes for preparing the compounds.Type: ApplicationFiled: October 19, 2012Publication date: September 18, 2014Inventors: Thomas John Bleisch, David Andrew Coates, Norman Earle Hughes, Scott Alan Jones, Bryan Hurst Norman
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Publication number: 20140271662Abstract: The invention provides compounds of the formula (I) having protein kinase B inhibiting activity: wherein A is a saturated hydrocarbon linker group containing from 1 to 7 carbon atoms, the linker group having a maximum chain length of 5 atoms extending between R1 and NR2R3 and a maximum chain length of 4 atoms extending between E and NR2R3, wherein one of the carbon atoms in the linker group may optionally be replaced by an oxygen or nitrogen atom; and wherein the carbon atoms of the linker group A may optionally bear one or more substituents selected from oxo, fluorine and hydroxy, provided that the hydroxy group when present is not located at a carbon atom ? with respect to the NR2R3 group and provided that the oxo group when present is located at a carbon atom ? with respect to the NR2R3 group; E is a monocyclic or bicyclic carbocyclic or heterocyclic group; R1 is an aryl or heteroaryl group; and R2, R3, R4 and R5 are as defined in the claims.Type: ApplicationFiled: February 14, 2014Publication date: September 18, 2014Applicants: Astex Therapeutics Ltd, Cancer Research Technology Limited, The Institute of Cancer Research: Royal Cancer HospitalInventors: Valerio BERDINI, Gordon SAXTY, Marinus Leendert VERDONK, Steven John WOODHEAD, Paul Graham WYATT, Robert George BOYLE, Hannah Fiona SORE, David Winter WALKER, Ian COLLINS, Robert DOWNHAM, Robin Arthur Ellis CARR
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Publication number: 20140274961Abstract: Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.Type: ApplicationFiled: March 15, 2013Publication date: September 18, 2014Applicant: Global Blood Therapeutics, Inc.Inventors: Brian W. Metcalf, Jason R. Harris, Zhe Li, Stephen L. Gwaltney, II
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Publication number: 20140256727Abstract: The present invention provides compositions and formulations of compounds having formula (I) and pharmaceutically acceptable derivatives thereof, wherein p, R1, R2 and B are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of any of a number of injuries, conditions or diseases in which HGF/SF or the activities thereof, or agonists or antagonists thereof have a therapeutically useful role. In addition, methods are provided for treating such diseases or diseases starting at a time after the onset of the injury, condition or disease.Type: ApplicationFiled: May 25, 2014Publication date: September 11, 2014Applicant: Angion Biomedica Corp.Inventors: Weizhong Cai, Prakash Narayan, Bijoy Panicker, David E. Smith
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Publication number: 20140256701Abstract: The present invention relates to phenalkylamine derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such phenalkylamine derivatives, and the use of such phenalkylamine derivatives for therapeutic purposes. The phenalkylamine derivatives are GlyT1 inhibitors.Type: ApplicationFiled: May 20, 2014Publication date: September 11, 2014Inventors: Frauke Pohlki, Udo Lange, Wilhelm Amberg, Michael Ochse, Berthold Behl, Wilfried Hornberger, Mario Mezler, Charles W. Hutchins, Sean Turner
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Publication number: 20140249137Abstract: The present invention relates to compounds useful as inhibitors of treating tuberculosis.Type: ApplicationFiled: October 31, 2013Publication date: September 4, 2014Applicant: Vertex Pharmaceuticals IncorporatedInventors: Tiansheng Wang, Brian Hanzelka, Ute Muh, Guy Bemis, Harmon J. Zuccola
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Publication number: 20140243339Abstract: This invention is in the field of pharmaceutical agents and specifically relates to compounds, compositions, uses and methods for treating cancer, by combining VEGF(R) inhibitors and inhibitors of HGF/SF:c-Met.Type: ApplicationFiled: February 28, 2014Publication date: August 28, 2014Applicant: Amgen Inc.Inventors: Teresa L. Burgess, Angela Coxon, Isabelle Dussault, Paula Kaplan-Lefko, Anthony J. Polverino, Darrin Beaupre
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Publication number: 20140243309Abstract: The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.Type: ApplicationFiled: September 21, 2012Publication date: August 28, 2014Inventors: Jason Brubaker, Christopher Dinsmore, Dawn Marie Hoffman, Joon Jung, Duan Liu, Scott Peterson, Tony Siu, Luis E. Torres, Hongjun Zhang, Zhongyong Wei, Feng Shi
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Publication number: 20140243338Abstract: The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same.Type: ApplicationFiled: February 28, 2014Publication date: August 28, 2014Inventors: Mimi L. Quan, Zilun Hu, Cailan Wang
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Publication number: 20140235641Abstract: The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.Type: ApplicationFiled: September 21, 2012Publication date: August 21, 2014Inventors: Jason Brubaker, Joshua Close, Tony Siu, Graham Frank Smith, Luis E. Torres, Hyun Chong Woo, Jonathan R. Young, Zhongyong Wei, Feng Shi
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Publication number: 20140235622Abstract: 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: January 28, 2014Publication date: August 21, 2014Applicant: Arena Pharmaceuticals, Inc.Inventors: Bradley Teegarden, Dennis Chapman, Juyi Choi, Konrad Feichtinger, Sangdon Han, Honnappa Jayakumar, Thuy-Anh Tran, Jay Xu, Ning Zou
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Publication number: 20140228358Abstract: The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.Type: ApplicationFiled: September 21, 2012Publication date: August 14, 2014Inventors: Jason Brubaker, Joshua T. Close, Joon Jung, Michelle Martinez, Catherine White, Kevin Wilson, Jonathan R. Young, Hongjun Zhang
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Publication number: 20140228348Abstract: The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.Type: ApplicationFiled: September 21, 2012Publication date: August 14, 2014Inventors: Jason Brubaker, Matthew Lloyd Childers, Matthew Christopher, Joshua T. Close, Jason David Katz, Joon Jung, Scott Peterson, Phieng Siliphaivanh, Tony Siu, Graham Frank Smith, Luis E. Torres, Hyun Chong Woo, Jonathan R. Young, Hongjun Zhang
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Publication number: 20140221362Abstract: The present application relates to the use of heterocyclic compounds, some of which are known, for controlling animal pests including arthropods and in particular insects, furthermore to novel heterocyclic compounds and to processes for their preparation.Type: ApplicationFiled: February 4, 2014Publication date: August 7, 2014Applicant: Bayer CropScience AGInventors: Thomas BRETSCHNEIDER, Martin Füßlein, Adeline Köhler, Friedrich August Mühlthau, Eva-Maria FRANKEN, Arnd VOERSTE
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Publication number: 20140221376Abstract: Pyridazine derivatives have unexpected drug properties as inhibitors of protein kinases and are useful in treating disorders related to abnormal protein kinase activities such as cancer.Type: ApplicationFiled: April 9, 2014Publication date: August 7, 2014Applicant: Xcovery Holding Company, LLCInventors: Congxin Liang, Zhigang Li
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Publication number: 20140213570Abstract: The present invention provides a compound of formula I or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: April 1, 2014Publication date: July 31, 2014Applicant: NOVARTIS AGInventors: Atwood Kim CHEUNG, Donovan Noel CHIN, Natalie DALES, Aleem FAZAL, Timothy HURLEY, John KERRIGAN, Gary O'BRIEN, Lei SHU, Robert SUN, Moo Je SUNG
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Patent number: 8791114Abstract: Novel dihydropyrazole derivatives of formula (I) wherein L, R, R3, R4, R5, R6, R7, X1, X2, X3, X4, Y, m and n have the meaning according to the claims, are positive allosteric modulators of the FSH receptor, and can be employed, inter alia, for the treatment of fertility disorders.Type: GrantFiled: June 26, 2012Date of Patent: July 29, 2014Assignee: Merck Patent GmbHInventors: Henry Yu, Thomas E. Richardson, Robert James Foglesong, Lizbeth Celeste DeSelm, Andreas Goutopoulos
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Publication number: 20140206660Abstract: The present invention provides phenyl-heteroaryl derivatives of Formula (I) and pharmaceutically acceptable salts thereof These compounds are useful in the treatment of RAGE-mediated diseases. The present invention further relates to methods for the preparation of compounds of Formula (I) and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising such compounds, and the use of such compounds and/or pharmaceutical compositions in treating RAGE-mediated diseases.Type: ApplicationFiled: March 26, 2014Publication date: July 24, 2014Applicant: TransTech Pharma, LLCInventors: Devi R. Gohimukkula, David Jones, Ghassan Qabaja, Jeff J. Zhu, Jeremy T. Cooper, William K. Banner, Kurt Sundermann, Muralidhar Bondlela, Mohan Rao, Pingzhen Wang, Raju B. Gowda, Robert C. Andrews, Suparna Gupta, Anitha Hari, Rongyuan Xie
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Patent number: 8785441Abstract: The present invention relates to certain 3-phenyl-pyrazole derivatives 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, reducing the risk of blood clot formation, asthma or symptoms thereof, agitation or a symptom, 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: GrantFiled: September 14, 2012Date of Patent: July 22, 2014Assignee: Arena Pharmaceuticals, Inc.Inventors: Bradley Teegarden, Yifeng Xiong, Sonja Strah-Pleynet, Honnappa Jayakumar, Peter I. Dosa, Konrad Feichtinger, Martin Casper, Juerg Lehmann, Robert M. Jones, David J. Unett, Jin Sun Karoline Choi
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Publication number: 20140200197Abstract: The compounds encompassed by Formula I include compounds which are HIV protease inhibitors and other compounds which can be metabolized in vivo to HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: ApplicationFiled: September 9, 2013Publication date: July 17, 2014Inventors: JOHN A. MCCAULEY, CHRISTIAN BEAULIEU, DAVID J. BENNETT, CHRISTOPHER J. BUNGARD, RONALD K. CHANG, SHELDON CRANE, THOMAS J. GRESHOCK, LI HAO, KATE HOLLOWAY, JESSE J. MANIKOWSKI, DANIEL MCKAY, CARMELA MOLINARO, OSCAR MIGUEL MORADEI, PHILIPPE G. NANTERMET, CHRISTIAN NADEAU, TUMMANAPALLI SATYANARAYANA, WILLIAM SHIPE, SANJAY KUMAR SINGH, VOUY LINH TRUONG, SIVALENKA VIJAYARADHI, PETER D. WILLIAMS, CATHERINE M. WISCOUNT
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Patent number: 8778939Abstract: The present invention relates to novel compounds that inhibit LRRK2 kinase activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases characterized by LRRK2 kinase activity, particularly Parkinson's disease and Alzheimer's disease.Type: GrantFiled: September 27, 2010Date of Patent: July 15, 2014Assignee: Glaxo Group LimitedInventors: Paula Louise Nichols, Andrew John Eatherton, Paul Bamborough, Karamjit Singh Jandu, Oliver James Philps, Daniele Andreotti
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Patent number: 8772289Abstract: N-Thio-anthranilamid compounds of formula (I) wherein A is A1 wherein the variables and the indices are as defined per the description, processes for preparing the compounds I, pesticidal compositions comprising compounds I, use of compounds I for the control of insects, acarids or nematodes, and methods for treating, controlling, preventing or protecting animals against infestation or infection by parasites by use of compounds of formula I.Type: GrantFiled: November 20, 2012Date of Patent: July 8, 2014Assignee: BASF SEInventors: Thomas Schmidt, Michael Puhl, Joachim Dickhaut, Henricus Maria Martinus Bastiaans, Michael Rack, Deborah L. Culbertson, Douglas D. Anspaugh, Franz-Josef Braun, Toni Bucci, Henry Van Tuyl Cotter, David G. Kuhn, Hassan Oloumi-Sadeghi
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Publication number: 20140187540Abstract: Compounds, compositions, kits and methods for treating conditions related to neurodegeneration or ocular disease, are disclosed.Type: ApplicationFiled: February 15, 2012Publication date: July 3, 2014Applicant: The Johns Hopkins UniversityInventors: Donald J. Zack, Cynthia Berlinicke, Laszlo Hackler, Zhiyong Yang, Joseph P. Steiner, Tomas Vojkovsky, Dana Ferraris, Barbara S. Slusher, James Inglese
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Publication number: 20140179670Abstract: The present invention provides: an uracil derivative represented by general formula (I) or a physiologically acceptable salt thereof (in the formula, R1 represents a hydrogen atom, a C1-10 alkyl group, a C2-6 alkene group or a 3- to 6-membered saturated or 4- to 6-membered unsaturated aliphatic ring group which may contain 1 to 2 hetero atoms independently selected from the group consisting of N, O and S; R2 represents a hydrogen atom, a halogen atom, a cyano group, —NRcRd, —N?CHN(CH3)2, or an C1-3 alkyl group; Ar1 and Ar2 independently represent a 5- to 6-membered aromatic ring group which may contain 1 to 3 hetero atoms independently selected from the group consisting of N, O and S; and L represents a 6-membered aromatic ring group which may contain 1 to 4 nitrogen atoms, a pyrazole group, a triazole group, or an imidazole group); and a therapeutic agent or prophylactic agent for various inflammatory diseases associated with elastase, comprises the compound or the like as an active ingredient.Type: ApplicationFiled: July 31, 2012Publication date: June 26, 2014Applicant: DAINIPPON SUMITOMO PHARMA CO., LTD.Inventors: Tomoya Shiro, Masanori Tobe, Katsumi Kubota, Yosuke Takanashi, Tomoaki Nakamura, Toshihiko Sone
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Publication number: 20140179702Abstract: The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity.Type: ApplicationFiled: October 15, 2013Publication date: June 26, 2014Inventors: Andreas Kling, Katja Jantos, Helmut Mack, Achim Möller, Wilfried Hornberger, Gisela Backfisch, Yanbin Lao, Marjoleen Nijsen
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Publication number: 20140163017Abstract: In one aspect, the invention relates to substituted (E)-N?-(1-phenylethylidene)benzohydrazide analogs, derivatives thereof, and related compounds, which are useful as inhibitors of lysine-specific histone demethylase, including LSD1; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions to treat disorders associated with dysfunction of the LSD1. 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: June 19, 2013Publication date: June 12, 2014Applicant: UNIVERSITY OF UTAHInventors: Hariprasad Vankayalapati, Venkataswamy Sorna, Steven L. Warner, Bret Stephens, David J. Bearss, Sunil Sharma
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Publication number: 20140163001Abstract: Provided is a heterocyclic compound having an ROR?t inhibitory activity.Type: ApplicationFiled: July 27, 2012Publication date: June 12, 2014Applicant: Takeda Pharmaceutical Company LimitedInventors: Satoshi Yamamoto, Junya Shirai, Atsuko Ochida, Yoshiyuki Fukase, Yoshihide Tomata, Ayumu Sato, Shotaro Miura, Kazuko Yonemori, Ryokichi Koyama
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Publication number: 20140163032Abstract: 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: February 18, 2014Publication date: June 12, 2014Applicant: ARENA PHARMACEUTICALS, INC.Inventors: 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: 20140163031Abstract: The present invention relates to compounds of Formula (I), wherein X1, X2, X3, X4, R1, R2, R3, and Q are as defined herein, useful as N-type calcium channel blockers.Type: ApplicationFiled: August 16, 2013Publication date: June 12, 2014Applicant: Janssen Pharmaceutica NVInventors: Mark Wall, Nalin Subasinghe, Zhihua Sui
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Publication number: 20140142106Abstract: The present invention provides a method for treating, preventing or reducing peritoneal fibrosis comprising administering to a subject in need thereof a pharmacologically effective dose of a type I cannabinoid receptor (CB1R) antagonist or a type II cannabinoid receptor (CB2R) agonist. Also provided is a dialysis fluid for treating, preventing or reducing peritoneal fibrosis comprising electrolytes, an osmotic agent, a physiologically acceptable pH solution, and a pharmacologically effective dose of a CB1R antagonist or a CB2R agonist.Type: ApplicationFiled: January 11, 2013Publication date: May 22, 2014Applicant: TAIPEI VETERANS GENERAL HOSPITALInventors: Chih-Yu Yang, An-Hang Yang
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Publication number: 20140142097Abstract: Compounds of the formula (I) in which R, R1 and X have the meanings indicated in claim 1, are inhibitors of TBK1 and IKK? and can be employed, inter alia, for the treatment of cancer and inflammatory diseasesType: ApplicationFiled: April 11, 2012Publication date: May 22, 2014Applicant: Merck Patent GmbHInventors: Guenter Hoelzemann, Hans-Michael Eggenweiler, Srinivasa R. Karra
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Publication number: 20140142088Abstract: The present invention is directed to novel pyridazinone derivatives that mediate enzymatic activity. In particular, the compounds may be effective in the treatment of diseases or disease states related to the activity of the histamine H3 receptor, including, for example, neurodegenerative disorders, sleep/wake disorders, attention deficit hyperactivity disorder and cognition.Type: ApplicationFiled: November 18, 2013Publication date: May 22, 2014Applicant: CEPHALON, INC.Inventors: Edward R. Bacon, Thomas R. Bailey, Nadine C. Becknell, Sankar Chatterjee, Derek Dunn, Greg A. Hostetler, Robert L. Hudkins, Kurt A. Josef, Lars J.S. Knutsen, Ming Tao, Alison L. Zulli
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Publication number: 20140128385Abstract: The present invention relates to the use of BACE-2 inhibitors and pharmaceutical compositions comprising BACE-2 inhibitors for treating metabolic disorders related to decreased ? cell mass and/or function.Type: ApplicationFiled: January 13, 2012Publication date: May 8, 2014Inventor: Heinrich Ruegger
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Publication number: 20140128396Abstract: Compounds selected from the group according to Claim 1 are inhibitors of tyrosine kinases, in particular of Met kinase, and can be employed, inter alia, for the treatment of tumours.Type: ApplicationFiled: January 7, 2014Publication date: May 8, 2014Applicant: Merck Patent GmbHInventors: Oliver SCHADT, Dieter DORSCH, Frank STIEBER, Andree BLAUKAT
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Patent number: 8703768Abstract: The invention is concerned with novel nitrogen-containing heteroaryl compounds of formula (I) wherein A1, A2, R1, R2, R3, R4, R5 and R6 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDE10A and can be used as therapeutics.Type: GrantFiled: June 2, 2011Date of Patent: April 22, 2014Assignee: Hoffmann-La Roche Inc.Inventors: Konrad Bleicher, Alexander Flohr, Katrin Groebke Zbinden, Felix Gruber, Matthias Koerner, Bernd Kuhn, Jens-Uwe Peters, Rosa Maria Rodriguez-Sarmiento
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Patent number: 8703770Abstract: The present invention is directed to pyridazine carboxamide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.Type: GrantFiled: October 26, 2009Date of Patent: April 22, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Paul J. Coleman, Christopher D. Cox, Swati P. Mercer, Anthony J. Roecker, John D. Schreier
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Publication number: 20140107110Abstract: Disclosed are pyridinone compounds, method for preparing these compounds, and methods for treating fibrotic disorders.Type: ApplicationFiled: October 1, 2013Publication date: April 17, 2014Inventors: Brad Owen Buckman, John Beamond Nicholas, Johnnie Y. Ramphal, Kumaraswamy Emayan, Scott D. Seiwert
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Publication number: 20140107118Abstract: The invention relates to novel heterocyclic compounds of the formula in which all of the variables are as defined in the specification, pharmaceutical compositions thereof, combinations thereof, and their use as medicaments, particularly for the treatment of Alzheimer's Disease or diabetes via inhibition of BACE-1 or BACE-2.Type: ApplicationFiled: December 20, 2013Publication date: April 17, 2014Applicant: NOVARTIS AGInventors: Sangamesh BADIGER, Murali CHEBROLU, Konstanze HURTH, Sebastien JACQUIER, Rainer Martin LUEOEND, Rainer MACHAUER, Heinrich RUEEGER, Marina TINTELNOT-BLOMLEY, Siem Jacob VEENSTRA, Markus VOEGTLE
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Publication number: 20140107125Abstract: Pharmaceutical compositions and compounds are provided. The compounds of the invention demonstrate anti-proliferative activity, and may promote apoptosis in cells lacking normal regulation of cell cycle and death. In one embodiment of the invention, pharmaceutical compositions of the compounds in combination with a physiologically acceptable carrier are provided. The pharmaceutical compositions are useful in the treatment of hyperproliferative disorders, which disorders include tumor growth, lymphoproliferative diseases, angiogenesis. The compounds of the invention are substituted pyrazoles and pyrazolines.Type: ApplicationFiled: April 29, 2013Publication date: April 17, 2014Applicant: Dermira (Canada), Inc.Inventor: Dermira (Canada), Inc.
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Publication number: 20140107111Abstract: The invention refers to the use of a sigma ligand, particularly a sigma ligand of formula (I) to prevent and/or treat type-2 diabetes-associated pain and related symptoms.Type: ApplicationFiled: May 18, 2012Publication date: April 17, 2014Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.Inventors: Jose Miguel Vela Hernandez, Maria Isabel Martin Fontelles
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Patent number: 8691184Abstract: Inhibitors of Bcl-2/Bcl-xL and compositions containing the same are disclosed. Methods of using the Bcl-2/Bcl-xL inhibitors in the treatment of diseases and conditions wherein inhibition of Bcl-2/Bcl-xL provides a benefit, like cancers, also are disclosed.Type: GrantFiled: January 24, 2012Date of Patent: April 8, 2014Assignee: The Regents of the University of MichiganInventors: Shaomeng Wang, Haibin Zhou, Jianfang Chen, Angelo Aguilar, Jennifer L. Meagher, Duxin Sun, Chao-Yie Yang, Liu Liu, Longchuan Bai, Donna McEachem, Jeanne Stuckey, Xiaoqin Li
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Patent number: 8685975Abstract: Compounds that inhibit PDE10 are disclosed that have utility in the treatment of a variety of conditions, including (but not limited to) psychotic, anxiety, movement disorders and/or neurological disorders such as Parkinson's disease, Huntington's disease, Alzheimer's disease, encephalitis, phobias, epilepsy, aphasia, Bell's palsy, cerebral palsy, sleep disorders, pain, Tourette's syndrome, schizophrenia, delusional disorders, drug-induced psychosis and panic and obsessive-compulsive disorders. Pharmaceutically acceptable salts, stereoisomers, solvates and prodrugs of the compounds are also provided. Also disclosed are compositions containing a compound in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting PDE10 in a warm-blooded animal in need of the same.Type: GrantFiled: November 16, 2012Date of Patent: April 1, 2014Assignee: Omeros CorporationInventors: Neil S. Cutshall, Jennifer Lynn Gage, Thomas Neil Wheeler, Thomas L. Little
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Patent number: 8685964Abstract: The present application relates to the use of heterocyclic compounds, some of which are known, for controlling animal pests including arthropods and in particular insects, furthermore to novel heterocyclic compounds and to processes for their preparation.Type: GrantFiled: October 12, 2010Date of Patent: April 1, 2014Assignee: Bayer CropScience AGInventors: Thomas Bretschneider, Martin Füβlein, Adeline Köhler, Friedrich August Mühlthau, Eva-Maria Franken, Arnd Voerste
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Patent number: 8685974Abstract: Thienylpyri(mi)dinylazole of the formula (I) in which R1 to R8 and X1 have the meanings given in the description, and agrochemically active salts, to their use and to methods and compositions for controlling phytopathogenic harmful fungi in and/or on plants or in and/or on seed of plants and for reducing mycotoxins in plants and parts of the plants, to processes for preparing such compounds and compositions and treated seed and also to their use for controlling phytopathogenic harmful fungi in agriculture, horticulture, forestry, in animal husbandry, in the protection of materials, in the domestic and hygiene field and for the reduction of mycotoxins in plants and parts of the plants.Type: GrantFiled: December 21, 2010Date of Patent: April 1, 2014Assignee: Bayer CropScience AGInventors: Alexander Sudau, Mazen Es-Sayed, Julia Neumann, Catherine Sirven, Jürgen Benting, Christoph Andreas Braun, Ruth Meissner, Anne-Sophie Rebstock, Samir Bennabi, Philippe Desbordes, Arounarith Tuch, Philippe Rinolfi, Stephane Brunet, Hiroyuki Hadano, Marie-Claire Grosjean-Cournoyer