1,3,4-oxadiazoles (including Hydrogenated) Patents (Class 548/143)
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Patent number: 8772323Abstract: The present invention relates to pyridazinone derivatives of general formula I, wherein the groups A, G and R1 are as defined in the application, the tautomers thereof, stereoisomers thereof, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.Type: GrantFiled: May 6, 2011Date of Patent: July 8, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Matthias Grauert, Remko Bakker, Steffen Breitfelder, Frank Buettner, Peter Eickelmann, Thomas Fox, Marc Grundl, Thorsten Lehmann-Lintz, Wolfgang Rist
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Patent number: 8772288Abstract: The present disclosure is directed to new inhibitors of the p38 mitogen-activated protein kinase having the general formula (I), processes for preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.Type: GrantFiled: April 3, 2009Date of Patent: July 8, 2014Assignee: Almirall, S.A.Inventors: Paul Robert Eastwood, Jacob Gonzalez Rodriguez, Bernet Vidal Juan, Nuria Aguilar Izquierdo
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Publication number: 20140187581Abstract: The present invention relates to novel compounds of formula (I), and their pharmaceutically acceptable salts and compositions containing them. The present invention also relates to a process for the preparation of above said novel compounds, and their pharmaceutically acceptable salts. The compounds of formula (I) are useful in the treatment of various disorders that are related to 5-HT4 receptors.Type: ApplicationFiled: January 5, 2012Publication date: July 3, 2014Applicant: SUVEN LIFE SCIENCES LIMITEDInventors: Ramakrishna Nirogi, Abdul Rasheed Mohammed, Suresh Yarlagadda, Srinivasa Rao Ravella, Anil Karbhari Shinde, Ramasastri Kamphampati, Praveen Kumar Roayapalley, Pradeep Jayarajan, Gopinadh Bhyrapuneni, Sriramachandra Murthy Patnala, Jyothsna Ravula, Venkateswarlu Jasti
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Publication number: 20140179735Abstract: A variety of benzofurans and indole derivatives some with an alkynyl linker are disclosed herein. These compounds are not highly charged at physiological pH and have good bioavailability characteristics. These compounds exhibit selective or at least preferential affinity for the active sites of various sub-sets of protein tyrosine phosphatases. Some of these compounds are excellent inhibitors of Mycobacterium protein tyrosine phosphatase B (mPTPB) a protein tyrosine phosphatase expressed in Mycobacterium tuberculosis and characterized as a virulence factor in the causal agent of tuberculosis. Accordingly, many of these compounds and pharmaceutically acceptable salts thereof are useful for the treatment of diseases such as tuberculosis.Type: ApplicationFiled: April 25, 2012Publication date: June 26, 2014Inventors: Zhong-Yin Zhang, Yantao He, Li-Fan Zeng
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Publication number: 20140179695Abstract: The present invention provides a compound which is useful as an active ingredient of a pharmaceutical composition, in particular, a pharmaceutical composition for preventing or treating diseases or conditions associated with and/or mediated by ?-secretase activity, hydrolysis of a ?-secretase site of a ?-amyloid precursor protein, and/or ?-amyloid protein accumulation, including a pharmaceutical composition for preventing or treating diseases including, but not limited to, Glaucoma, MCI (Mild cognitive impairment) or Alzheimer's disease, especially, Alzheimer's disease.Type: ApplicationFiled: February 27, 2014Publication date: June 26, 2014Applicants: CoMentis, Inc., ASTELLAS PHARMA INC.Inventors: Ryosuke MUNAKATA, Makoto INOUE, Hiroaki TOMINAGA, Shingo YAMASAKI, Yasuhiro SHIINA, Kiyohiro SAMIZU, Hisao HAMAGUCHI, Lin HONG
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Publication number: 20140171313Abstract: This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.Type: ApplicationFiled: December 18, 2013Publication date: June 19, 2014Applicant: DOW AGROSCIENCES LLCInventors: William C. Lo, James E. Hunter, Gerald B. Watson, Akshay Patny, Pravin S. Iyer, Joshodeep Boruwa
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Patent number: 8754113Abstract: A compound represented by the formula: or its pharmaceutically acceptable salt. Ring A is aromatic carbocycle or aromatic heterocycle, Z is —O— or —S—, R1 is hydrogen, halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl or the like, R2 and R3 are each independently hydrogen, halogen, hydroxy or the like, R4 is a group represented by the formula: —(CR6R7)n—R8, R6 and R7 are each independently hydrogen, halogen, hydroxy or the like, n is an integer of 0 to 3, R8 is carboxy, cyano, substituted or unsubstituted alkyl or the like, Rx is halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl or the like, and m is an integer of 0 to 3.Type: GrantFiled: December 14, 2010Date of Patent: June 17, 2014Assignee: Shionogi & Co., Ltd.Inventors: Koji Masuda, Shiro Kida, Naoki Yoshikawa, Manabu Katou, Terukazu Kato, Mado Nakajima, Eiichi Kojima, Mitsuhiro Yonehara
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Patent number: 8735430Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.Type: GrantFiled: September 26, 2012Date of Patent: May 27, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Alessandra Bartolozzi, Eugene Richard Hickey, Doris Riether, Lifen Wu, Renee M. Zindell, Nigel James Blumire, Monika Ermann, Edward Thomas Glenn, Someina Khor, Przemyslaw Zawadzki
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Patent number: 8722670Abstract: The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands, antagonists of the NR2B receptor and may be useful for the treatment of various disorders of the central nervous system.Type: GrantFiled: September 26, 2012Date of Patent: May 13, 2014Assignee: Bristol-Myers Squibb CompanyInventors: Dalton King, Richard E. Olson, John E. Macor, Imadul Islam, Srinivasan Thangathirupathy, Jayakumar Sankara Warrier
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Publication number: 20140121196Abstract: A compound that inhibits interaction between, murine double minute 2 (Mdm2) protein and p53 protein and exhibits anti-tumor activity is provided. The present invention provides a dispiropyrrolidine derivative represented by the following formula (1), which has various substituents, inhibits interaction between Mdm2 protein and p53 protein and exhibits anti-tumor activity, wherein R1, R2, R3, ring A, and ring B in formula (1) respectively have the same meanings as defined in the specification.Type: ApplicationFiled: November 14, 2013Publication date: May 1, 2014Applicant: Daiichi Sankyo Company, LimitedInventors: Yuuichi Sugimoto, Kouichi Uoto, Takanori Wakabayashi, Masaki Miyazaki, Masaki Setoguchi, Toru Taniguchi, Keisuke Yoshida, Akitake Yamaguchi, Shoko Yoshida
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Patent number: 8685958Abstract: Disclosed herein are azetidinyl compounds of formula I, as described herein, pharmaceutical compositions comprising an azetidinyl compound, and a method of using an azetidinyl compound in the treatment or prophylaxis of a melanin-concentrating hormone related disease or condition.Type: GrantFiled: July 13, 2012Date of Patent: April 1, 2014Assignee: AstraZeneca ABInventor: Lars Anders Mikael Johansson
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Patent number: 8686159Abstract: An oxadiazole derivative represented by the following general formula (G1) is synthesized and applied to the light emitting element, Am; wherein Am is a substituent represented by a general formula (Am1), (Am2), or (Am3); each of ?, ?1, and ?2 represents an arylene group having 6 to 25 carbon atoms; each of Ar1 to Ar6 represents an aryl group having 6 to 25 carbon atoms; each of R1 to R3 represents hydrogen, an alkyl group having 1 to 4 carbon atoms, or an aryl group having 6 to 25 carbon atoms; and R4 represents an alkyl group having 1 to 4 carbon atoms or an aryl group having 6 to 25 carbon atoms.Type: GrantFiled: February 28, 2013Date of Patent: April 1, 2014Assignee: Semiconductor Energy Laboratory Co., Ltd.Inventors: Hiroko Murata, Harue Nakashima, Sachiko Kawakami, Nobuharu Ohsawa, Ryoji Nomura, Satoshi Seo
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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: 8680090Abstract: The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.Type: GrantFiled: July 8, 2013Date of Patent: March 25, 2014Assignee: Bristol-Myers Squibb CompanyInventors: James A. Johnson, Ji Jiang, Soong-Hoon Kim, Zulan Pi, Jennifer X. Qiao, George O. Tora, Tammy C. Wang, Heather Finlay
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Publication number: 20140080705Abstract: N-(1,3,4-Oxadiazol-2-yl)arylcarboxamides of the general formula (I) are described as herbicides. In this formula (I) A is nitrogen or CY. R, X, Y and Z are each radicals such as hydrogen, organic radicals such as alkyl, and other radicals such as halogen.Type: ApplicationFiled: March 21, 2012Publication date: March 20, 2014Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Arnim Köehn, Hartmut Ahrens, Ralf Braun, Simon Dörner-Rieping, Stefan Lehr, Ines Heinemann, Isolde Häuser-Hahn, Elmar Gatzweiler, Christoper Hugh Rosinger
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Publication number: 20140065103Abstract: A compound is selected from the structural formulae depicted in FIG. 1 or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound selected from the structural formulae depicted in FIG. 1 or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier of excipient. A method of treating a HCV infection in a subject comprises administering to the subject a therapeutically effective amount of selected from the structural formulae depicted in FIG. 1 or a pharmaceutically acceptable salt thereof. A method of inhibiting or reducing the activity of HCV polymerase in a subject or in a biological in vitro sample comprises administering to the subject or to the sample a therapeutically effective amount of selected from the structural formulae depicted in FIG. 1 or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: February 14, 2013Publication date: March 6, 2014Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventor: VERTEX PHARMACEUTICALS INCORPORATED
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Publication number: 20140051709Abstract: Disclosed is a compound for treatment of Myotonic Dystrophy type 1 having the formula: Wherein X is selected from the group consisting of O, N, C, or S, Y is a homo- or heteroatomic 5-membered ring comprising one or more atoms selected from the group consisting of N, O, S, and C, Z is an optionally substituted aryl group or optionally substituted heteroaryl, including but not limited to halogenated benzenes, pyridines, substituted benzene, substituted pyridine, R2=hydroxy, acyl, alkoxyl, esters, ethers, cyclic ethers, and lactones, R3=H, alkyl, an optionally substituted alkyl, aliphatic ether, ester, cyclic unsaturated and aromatic ring groups, and R1, R4 and R5 are independently selected from the group consisting of hydrogen, halogen, alkyl, and alkoxyl or a pharmaceutically or cosmetically acceptable salt, solvate, or hydrate thereof.Type: ApplicationFiled: August 16, 2012Publication date: February 20, 2014Applicant: UNIVERSITY OF SOUTHERN CALIFORNIAInventors: Sita REDDY, Lucio Comai, Nouri Neamati
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Publication number: 20140051862Abstract: This invention provides new compounds having NPY Y5 antagonistic activity. The present inventors found that a compound of the formula (I): wherein R1 is substituted or unsubstituted alkyl or the like; p, q and r are each independently 0 or 1; ring A is oxadiazole; and R2 is substituted or unsubstituted alkyl or the like, has NPY Y5 antagonistic activity.Type: ApplicationFiled: April 25, 2012Publication date: February 20, 2014Applicant: Shionogi & Co., Ltd.Inventors: Kyohei Hayashi, Yuusuke Tamura, Naoki Omori
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Patent number: 8653127Abstract: The present invention provides substituted pyrazolo-heterocycles having the general structure of formula I The structures of rings A and B and substituents Ra, Rb and Rc are described in the specification. Also provided are pharmaceutically acceptable salts, acid salts, hydrates, solvates and stereoisomers of the compounds of formula I. The compounds are useful as modulators of cannabinoid receptors and for the prophylaxis, treatment and inhibition of cannabinoid receptor-associated diseases and conditions, such as pain, inflammation and pruritis.Type: GrantFiled: January 14, 2010Date of Patent: February 18, 2014Assignee: Cara Therapeutics, Inc.Inventor: Robert Zhiyong Luo
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Publication number: 20140045811Abstract: The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.Type: ApplicationFiled: July 18, 2013Publication date: February 13, 2014Inventors: Heather Finlay, Ji Jiang, Soong-Hoon Kim, Brandon Parkhurst, Jennifer X. Qiao, Tammy C. Wang, Zulan Pi, George O. Tora, John Lloyd, James A. Johnson
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Patent number: 8642632Abstract: This invention provides compounds as described herein or pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising a compound as described herein or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable excipient, methods of modulating the androgen receptor using the compounds or compositions described herein, methods of treating diseases beneficially treated by an androgen receptor modulator (e.g., sarcopenia, prostate cancer, contraception, type 2 diabetes related disorders or diseases, anemia, depression, and renal disease) using the compounds and compositions described herein and processes for making compounds described herein and intermediates useful in the preparation of same.Type: GrantFiled: July 1, 2011Date of Patent: February 4, 2014Assignee: Radius Health, Inc.Inventor: Chris P. Miller
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Patent number: 8629167Abstract: This invention provides compounds of formulas I, Ia, Ib, Ic, Id, Ie, If or Ig or salts thereof, pharmaceutical compositions comprising a compound of formulas I, Ia, Ib, Ic, Id, If or Ig and a pharmaceutically acceptable excipient, methods of modulating the androgen receptor, methods of treating diseases beneficially treated by an androgen receptor modulator (e.g., sarcopenia, prostate cancer, contraception, type 2 diabetes related disorders or diseases, anemia, depression, and renal disease) and processes for making compounds of formulas I, Ia, Ib, Ic, Id, Ie, If or Ig and intermediates useful in the preparation of same.Type: GrantFiled: August 9, 2012Date of Patent: January 14, 2014Assignee: Radius Health, Inc.Inventor: Chris P. Miller
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Publication number: 20140011799Abstract: The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.Type: ApplicationFiled: July 8, 2013Publication date: January 9, 2014Inventors: James A. Johnson, Ji Jiang, Soong-Hoon Kim, Zulan Pi, Jennifer X. Qiao, George O. Tora, Tammy C. Wang, Heather Finlay
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Publication number: 20140005164Abstract: The present invention relates to novel compounds of formula (I): as herein described and pharmaceutical compositions thereof. The compounds of formula (I) have inhibitory effect on the Wnt pathway and are therefore useful in the preparation of a medicament, in particular for the treatment of cancer.Type: ApplicationFiled: March 23, 2012Publication date: January 2, 2014Applicant: Siena Biotech S.p.A.Inventors: Maurizio Varrone, Massimiliano Travagli, Giacomo Minetto, Lucia Cesari, Simone Galeazzi, Andrea Caricasole, Antonio Chiumiento, Massimiliano Salerno
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Publication number: 20130345120Abstract: The present invention relates to a compound of Formula (I): or a pharmaceutically acceptable salt thereof, corresponding pharmaceutical compositions, compound preparation and treatment methods directed to bacterial infections and inhibition of bacterial peptide deformylase (PDF) activity.Type: ApplicationFiled: March 9, 2012Publication date: December 26, 2013Applicant: Glaxosmithkline LLCInventors: Kelly M. Aubart, Andrew B. Benowitz, Yuhong Fang, James Hoffman, Joseph M. Karpinski, Andrew Nicholson Knox, Xiangmin Liao, Donghui Qin, Dongchuan Shi, Jared T. Spletstoser
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Publication number: 20130345419Abstract: Provided are novel compounds that bind to FKBP12 or pharmaceutically acceptable salts thereof, as well as new therapeutics useful in the prevention or treatment of alopecia which comprise those compounds or pharmaceutically acceptable salts thereof. Specifically, compounds represented by formula (1) [where R1 represents either the following formula (2) or (3)] or pharmaceutically acceptable salts thereof are provided.Type: ApplicationFiled: March 15, 2012Publication date: December 26, 2013Applicant: TAISHO PHARMACEUTICAL CO., LTD.Inventors: Naoya Ono, Shoichi Kuroda, Yoshihisa Shirasaki, Tetsuo Takayama, Yoshinori Sekiguchi, Fumihito Ushiyama, Yusuke Oka
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Publication number: 20130338196Abstract: Compounds are disclosed that are effective in inhibition of fatty acid amide hydrolase, an enzyme responsible for catabolism of endogenous cannabinoids such as anandamide. The compounds are useful as analgesic compounds and as sleep-inducing compounds, that can be orally administered, and that can have a relatively long duration of effect. Methods of preparation of the compounds are also provided. The compounds are conformationally constrained analogs of heterocyclylketones such as oxazolylketones.Type: ApplicationFiled: February 3, 2012Publication date: December 19, 2013Applicant: The Scripps Research InstituteInventor: Dale L. Boger
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Publication number: 20130331419Abstract: Disclosed are the compounds of the Formula (I) as well as pharmaceutically acceptable salts thereof, which are useful for treating aldosterone-mediated diseases. The processes for preparing compounds of the Formula (I), the use for the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and the pharmaceutical compositions which comprise compounds of the formula (I) are disclosed too.Type: ApplicationFiled: January 19, 2012Publication date: December 12, 2013Inventors: Alejandro Crespo, Ping Lan, Rudrajit Mal, Anthony Ogawa, Hong Shen, Peter J. Sinclair, Zhongxiang Sun, Ellen K. Vande Bunte, Zhicai Wu, Kun Liu, Robert J. DeVita, Dong-Ming Shen, Min Shu, John Qiang Tan, Changhe Qi, Yuguang Wang, Richard Beresis
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Publication number: 20130296166Abstract: Compositions and processes for controlling nematodes are described herein, e.g., nematodes that infest plants or animals. The compounds include oxazoles, oxadiazoles and thiadiazoles.Type: ApplicationFiled: April 3, 2013Publication date: November 7, 2013Inventors: Deryck J. Williams, Matt W. Dimmic, William P. Haakenson, Al Wideman, Barry J. Shortt, Tim Cheeseright, Michael J. Crawford
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Publication number: 20130289058Abstract: The invention relates to compounds of formula (I): useful for treating disorders mediated by acyl coA-diacylglycerol acyl transferase 1 (DGAT1), e.g. metabolic disorders. The invention also provides methods of treating such disorders, and compounds and compositions etc. for their treatment.Type: ApplicationFiled: April 26, 2013Publication date: October 31, 2013Inventors: Sejal Patel, Justin Mao, Qian Lui, Rui Zheng, Tyler Harrison, Rohit Duvadie, Xin Chen, Frederic Zecri, Jay Larrow, Xuchun Zheng, Yizong Zhou, Jiong Ye, Yiping Ding, Yu Gai
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Publication number: 20130274256Abstract: Certain multi-cyclic compounds and compositions thereof are useful for reducing or inhibiting the growth of bacterial biofilms and for controlling bacterial biofilm infections. Such compounds and compositions are also useful in methods for reducing or inhibiting the growth of biofilms and for controlling bacterial biofilm infections involving biofilms.Type: ApplicationFiled: October 11, 2012Publication date: October 17, 2013Applicant: SEQUOIA SCIENCES, INC.Inventor: Sequoia Sciences, Inc.
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Patent number: 8546375Abstract: Disclosed herein are azetidinyl compounds of formula I, as described herein, pharmaceutical compositions comprising an azetidinyl compound, and a method of using an azetidinyl compound in the treatment or prophylaxis of a melanin-concentrating hormone related disease or condition.Type: GrantFiled: July 5, 2011Date of Patent: October 1, 2013Assignee: AstraZeneca ABInventors: Susanne Doris Margit Bökman-Winiwarter, Marlene Fredenwall, Carl Anders Hogner, Lars Anders Mikael Johansson, Robert Andrew Judkins, Lanna Li, Björn Christian Ingvar Löfberg, Sverker Von Unge
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Patent number: 8541453Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: GrantFiled: May 20, 2011Date of Patent: September 24, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Sara Sabina Hadida-Ruah, Peter Diederik Jan Grootenhuis, Mark Thomas Miller, Matthew Hamilton
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Publication number: 20130237702Abstract: A composition containing a compound represented by General Formula (I) below (see the definition in the specification for the symbols in the formula) or a salt thereof has an excellent CaSR agonistic effect and provides a pharmaceutical agent, a CaSR agonistic agent, a prophylactic or therapeutic agent for a disease that can be ameliorated through CaSR activation as well as seasonings and an agent for imparting kokumi.Type: ApplicationFiled: August 31, 2012Publication date: September 12, 2013Applicant: AJINOMOTO CO., INC.Inventors: Masayuki SUGIKI, Toru OKAMATSU, Tetsuo YANO, Shinya TANIGUCHI
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Publication number: 20130231342Abstract: The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula (I) as described and defined herein, and their use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection. Thus, in one specific aspect the invention relates to formulas (II), (III), (IV), (V), (VI), (VII), (VIII), (IX).Type: ApplicationFiled: July 27, 2011Publication date: September 5, 2013Applicant: Oryzon Fenomics S.A.Inventors: Alberto Ortega Muñoz, Matthew Colin Thor Fyfe, Marc Martinell Pedemonte, Iñigo Tirapu Fernandez de la Cuesta, Maria de los Ángeles Estirate-Martinez
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Patent number: 8524751Abstract: The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): and salts thereof. The compounds of the invention are inhibitors of kinase activity, in particular PI3-kinase activity.Type: GrantFiled: March 5, 2010Date of Patent: September 3, 2013Assignee: GlaxoSmithKline Intellecutual Property DevelopmentInventors: Julie Nicole Hamblin, Zoe Alicia Harrison, Paul Spencer Jones, Suzanne Elaine Keeling, Joelle Le, Christopher James Lunniss, Nigel James Parr
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Publication number: 20130225644Abstract: Lysine mimetic compounds having useful pharmacological activity such as antiarrhythmic activity and desirable bioavailability properties are disclosed.Type: ApplicationFiled: April 1, 2013Publication date: August 29, 2013Applicant: Zealand Pharma A/SInventor: Zealand Pharma A/S
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Publication number: 20130225591Abstract: The present invention is directed to novel kinase inhibitors of general formula (I) and pharmaceutically acceptable salts thereof, and to the use of the kinase inhibitors of general formula (I) for treating diseases or disorders in which tau phosphorylation and cell cycle regulation is implicated, such as Alzheimer's Disease and cancer.Type: ApplicationFiled: September 14, 2010Publication date: August 29, 2013Inventors: Michelle R. Machacek, Sean P. Ahearn, Eric Romeo, Tony Siu, Stephanie Chichetti, Gabriela de Almeida, Alexey A. Rivkin
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Publication number: 20130217702Abstract: The present invention relates to the indole derivatives of formula (I), wherein R1-R6 and X are defined in the claims and optical antipodes or racemates and/or salts thereof which are selective antagonists of bradykinin B1 to process for producing these compounds, pharmacological compositions containing them and to their use in therapy or prevention of painful and inflammatory conditions.Type: ApplicationFiled: November 4, 2011Publication date: August 22, 2013Inventors: Gyula Beke, Gyula Attila Bényei, István Borza, Éva Bozó, Sándor Farkas, Katalin Hornok, Andrea Papp, István Vágó, Mónika Vastag
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Patent number: 8513436Abstract: Disclosed herein are novel antioxidant inflammation modulators, including those of the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds. Methods and intermediates useful for making the compounds, and methods of using the compounds and compositions thereof are also provided.Type: GrantFiled: December 19, 2011Date of Patent: August 20, 2013Assignee: Reata Pharmaceuticals, Inc.Inventors: Eric Anderson, Gary L. Bolton, Bradley Caprathe, Xin Jiang, Chitase Lee, William H. Roark, Melean Visnick
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Publication number: 20130197011Abstract: Substituted phenyl-3-aza-bicyclo[3.1.0]hex-3-yl-methanones which are glycine transporter-1 (GlyT1) inhibitors. These are useful for the treatment of schizophrenia, Alzheimer's Disease and other neurological and psychiatric disorders.Type: ApplicationFiled: July 27, 2012Publication date: August 1, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Riccardo GIOVANNINI, Barbara BERTANI, Marco FERRARA, Iain LINGARD, Rocco MAZZAFERRO, Holger ROSENBROCK
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Patent number: 8492415Abstract: The present invention relates to novel heterocyclic compounds, including oxadiazole compounds, pharmaceutical compositions and their use in the inhibition of reverse transcriptase and the treatment of HIV (1 and 2) infections, AIDS and ARC and other viral infections.Type: GrantFiled: July 2, 2008Date of Patent: July 23, 2013Assignee: Yale UniversityInventor: William L. Jorgensen
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Publication number: 20130184250Abstract: Disclosed herein are azetidinyl compounds of formula I, as described herein, pharmaceutical compositions comprising an azetidinyl compound, and a method of using an azetidinyl compound in the treatment or prophylaxis of a melanin-concentrating hormone related disease or condition.Type: ApplicationFiled: July 13, 2012Publication date: July 18, 2013Applicant: ASTRAZENECA ABInventor: Lars Anders Mikael Johansson
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Patent number: 8486297Abstract: The present invention relates to thiophene derivatives, to processes and intermediates for the preparation thereof, to the use thereof for optical, electro-optical and electronic purposes, in particular in liquid-crystal (LC) media and LC displays, and to LC media and LC displays comprising same.Type: GrantFiled: February 3, 2010Date of Patent: July 16, 2013Assignee: Merck Patent GmbHInventors: Axel Jansen, Detlef Pauluth, Harald Hirschmann, Markus Czanta
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Publication number: 20130172384Abstract: This invention relates to the use of triazolone and triazolethione derivatives for the modulation, notably the inhibition of the activity or function of fatty acid synthase (FAS). Suitably, the present invention relates to the use of triazolones and triazolethiones in the treatment of cancer.Type: ApplicationFiled: September 15, 2011Publication date: July 4, 2013Inventors: Nicholas D. Adams, Christopher Joseph Aquino, Jonathan M. Ghergurovich, David Lee Musso, Cynthia A. Parrish
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Patent number: 8476302Abstract: The present invention is directed to ?-ketoamide derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by endothelial lipase, for example, cardiovascular disorders.Type: GrantFiled: September 26, 2011Date of Patent: July 2, 2013Assignee: Janssen Pharmaceutica N.V.Inventors: Michael N. Greco, Margery A. Connelly, Shyamali Ghosh, Dennis J. Hlasta, Edward C. Lawson, Eric Strobel, Michele A. Weidner-Wells, Hong Ye
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Publication number: 20130165433Abstract: The present invention is directed to compounds for use in the treatment or prevention of influenza virus infection.Type: ApplicationFiled: September 6, 2011Publication date: June 27, 2013Applicant: GlaxoSmithKline Intellectual Property Development LimitedInventors: Ian Robert Baldwin, Kenneth David Down, Paul Faulder, Simon Gaines, Julie Nicole Hamblin, Zoe Alicia Harrison, Katherine Louise Jones, Paul Spencer Jones, Suzanne Elaine Keeling, Joelle Le, Christopher James Lunniss, Charlotte Jane Mitchell, Nigel James Parr, Timothy John Ritchie, John Edward Robinson, Juliet Kay Simpson, Christopher Alan Paul Smethurst, Yoshiaki Washio
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Patent number: 8470819Abstract: This invention provides compounds of Formula I which are PAFR antagonists: I and the pharmaceutically acceptable salts thereof. The compounds are useful for treating PAF-mediated disorders, and can be used in methods for treating atherosclerosis and preventing or reducing risk for atherosclerotic disease events. The compounds are also useful for treating or ameliorating pain, e.g. inflammatory pain and/or nociceptive pain, and for treating or ameliorating autoimmune and/or inflammatory diseases, among other conditions.Type: GrantFiled: October 26, 2009Date of Patent: June 25, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Lin Chu, Anthony Ogawa, Hyun O. Ok, Feroze Ujjainwalla
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Publication number: 20130158075Abstract: The present invention relates to heterocyclic compounds of formula 1, in all their stereoisomeric and tautomeric forms; and their pharmaceutically acceptable salts, solvates, polymorphs, prodrugs, carboxylic acid isosteres and N-oxides. The invention also relates to processes for the manufacture of the heterocyclic compounds and to pharmaceutical compositions containing them. The said compounds and their pharmaceutical compositions are useful in the prevention and treatment of diseases or disorders mediated by diacylglycerol acyltransferase (DGAT), particularly DGAT1. The present invention further provides a method of treatment of such diseases or disorders by administering a therapeutically effective amount of said compounds or their pharmaceutical compositions, to a mammal in need thereof.Type: ApplicationFiled: August 31, 2011Publication date: June 20, 2013Applicant: PIRAMAL ENTERPRISES LIMITEDInventors: Rajiv Sharma, Kishorkumar Shivajirao Kadam, Ravindra Dnyandev Jadhav, Shivaji Sadashiv Kandre, Amol Gupte
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Publication number: 20130150392Abstract: The compound (I) or a salt thereof has an excellent controlling activity against pests. Then the compound (I) or a salt thereof is useful for an active ingredient of a pesticidal composition.Type: ApplicationFiled: February 8, 2013Publication date: June 13, 2013Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventor: SUMITOMO CHEMICAL COMPANY, LIMITED