Cyano Or -c(=x)-, Wherein X Is Chalcogen, Attached Directly Or Indirectly To The Oxazole Ring By Nonionic Bonding Patents (Class 548/236)
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Publication number: 20140206676Abstract: In one aspect, the invention relates to substituted 4-(1H-pyrazol-4-yl)benzyl analogs compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M1 (mAChR M1); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. 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: January 12, 2013Publication date: July 24, 2014Applicant: Vanderbilt UniversityInventors: Craig W. Lindsley, P. Jeffrey Conn, Michael R. Wood, Bruce J. Melancon, Michael S. Poslusney, James C. Tarr
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Publication number: 20140206706Abstract: The present invention provides a method for treating a thrombotic or an inflammatory disorder administering to a patient in need thereof a therapeutically effective amount of at least one compound of Formula (I) or Formula (V): or a stereoisomer or pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, R3, R4, R6, R11, X1, X2, and X3 are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also provides compounds within the scope of Formula I and relates to pharmaceutical compositions comprising these compounds.Type: ApplicationFiled: March 19, 2014Publication date: July 24, 2014Inventors: Jon J. Hangeland, Mimi L. Quan, Joanne M. Smallheer, Gregory S. Bisacchi, James R. Corte, Todd J. Friends, Zhong Sun, Karen A. Rossi, Cullen L. Cavallaro
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Publication number: 20140206880Abstract: A process for the preparation of 4-methyl-oxazole-5-carboxamide, an intermediate in the synthesis of pyridoxine, by reacting lower alkyl 4-methyl-oxazole-5-carboxy-late with a molar excess of anhydrous, liquid ammonia.Type: ApplicationFiled: May 31, 2012Publication date: July 24, 2014Applicant: DSM IP ASSETS B.V.Inventors: Werner Bonrath, Jocelyn Fischesser, Hongyan Shen
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Publication number: 20140194426Abstract: In one aspect, the invention relates to compounds having the formula: wherein: Ar, Z, R3, R4 and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: ApplicationFiled: October 24, 2013Publication date: July 10, 2014Applicant: THERAVANCE, INC.Inventors: Paul R. Fatheree, Ryan Hudson, Robert Murray McKinnell
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Publication number: 20140194443Abstract: The invention relates to pyrazolyl-based carboxamide compounds useful as ICRAC inhibitors, to pharmaceutical compositions containing these compounds and to these compounds for the use in the treatment and/or prophylaxis of diseases and/or disorders, in particular inflammatory diseases and/or inflammatory disorders.Type: ApplicationFiled: January 10, 2014Publication date: July 10, 2014Applicant: Grünenthal GmbHInventors: Sonja Nordhoff, Sebastian Wachten, Achim Kless, Felix Voss, Stefanie Ritter
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Publication number: 20140187596Abstract: The present invention provides a method of treating a patient suffering from pain or other FAAH mediated conditions by administering a fatty acid amide inhibiting amount of a compound represented by the formula: wherein R1 is H; R2 is a radical selected from the group consisting of H, hydrocarbyl and substituted hydrocarbyl; R3 is a radical selected from the group consisting of H, hydrocarbyl and substituted hydrocarbyl; X is CHCH, (CH2)n or O(CH2)n, wherein n is 0 or an integer of from 1 to 4; and W is O, S, or NR6, wherein R6 is selected from the group consisting of H and alkyl.Type: ApplicationFiled: May 23, 2012Publication date: July 3, 2014Applicant: ALLERGAN, INC.Inventors: David F. Woodward, Jose L. Martos, William R. Carling, Andrew D. Jones, Jenny W. Wang
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Patent number: 8765796Abstract: The present invention relates to novel compounds, methods, and formulations useful for the oral delivery of a GLP-1 compound or an MC4 agonist peptide.Type: GrantFiled: August 20, 2013Date of Patent: July 1, 2014Assignee: Emisphere Technologies, Inc.Inventors: Robert J. Herr, Louis N. Jungheim, John M. McGill, Kenneth J. Thrasher, Muralikrishna Valluri
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Publication number: 20140171474Abstract: The present invention relates to N-cycloalkyl-N-biphenylmethyl-carboxamide derivatives of formula (I) wherein A, Z1, Z2, Z3, X, n, Y and m represent various substituents, their process of preparation, preparation intermediate compounds, their use as fungicide active agents, particularly in the form of fungicide compositions and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositionsType: ApplicationFiled: February 19, 2014Publication date: June 19, 2014Inventors: Philippe DESBORDES, Ralf DUNKEL, Stephanie GARY, Marie-Claire GROSJEAN-COURNOYER, Benoit HARTMANN, Philippe RINOLFI, Jean-Pierre VORS, Rachel RAMA
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Patent number: 8748626Abstract: Disclosed are new substituted oxazole and thiazole compounds of Formula (I) and pharmaceutically acceptable salts, esters or prodrugs thereof, compositions of the derivatives together with pharmaceutically acceptable carriers, and uses thereof:Type: GrantFiled: April 13, 2011Date of Patent: June 10, 2014Assignee: Novartis AGInventors: Paul A. Barsanti, Yu Ding, Wooseok Han
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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: 8722901Abstract: Heteroaryl compounds, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or disorders mediated by Diacylglycerol acyltransferase (DGAT) enzyme, particularly DGAT-1 is described.Type: GrantFiled: November 1, 2010Date of Patent: May 13, 2014Assignee: Piramal Enterprises LimitedInventors: Ravindra Dnyandev Jadhav, Rajiv Sharma, Kishorkumar Shivajirao Kadam, Shivaji Sadashiv Kandre
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Publication number: 20140128437Abstract: The invention features a series of heterocyclic derivatives that inhibit tumor necrosis factor alpha (TNF-?) induced necroptosis. The heterocyclic compounds of the invention are described by Formulas (I) and (Ia)-(Ie) and are shown to inhibit TNF-? induced necroptosis in FADD-deficient variant of human Jurkat T cells. The invention further features pharmaceutical compositions featuring the compounds of the invention. The compounds and compositions of the invention may also be used to treat disorders where necroptosis is likely to play a substantial role.Type: ApplicationFiled: January 10, 2014Publication date: May 8, 2014Applicants: President and Fellows of Harvard College, TRUSTEES OF BOSTON UNIVERSITY, THE BRIGHAM AND WOMEN'S HOSPITAL, INC., Tufts UniversityInventors: Gregory D. Cuny, Xin Teng, Junying Yuan, Alexei Degterrev, John A. Proco, JR.
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Publication number: 20140121217Abstract: The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein A, Y, L, R1, W1 and W2 are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.Type: ApplicationFiled: January 2, 2014Publication date: May 1, 2014Applicant: Synta Pharmaceuticals Corp.Inventors: Shoujun Chen, Lijun Sun, Jun Jiang, Yu Xie
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Patent number: 8703761Abstract: The invention relates to compounds of formula (I): where A is an optionally substituted heteroaryl, 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: GrantFiled: July 14, 2009Date of Patent: April 22, 2014Assignee: Novartis AGInventors: Cornelia Jutta Forster, Young-Shin Kwak, Katsumasa Nakajima, Bing Wang
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Publication number: 20140107134Abstract: The invention relates to compounds of formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof wherein X, Y, A, Z, L and n are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions and immune disorders.Type: ApplicationFiled: September 27, 2013Publication date: April 17, 2014Applicant: Synta Pharmaceuticals Corp.Inventors: Yu Xie, Mats Holmqvist, Jerome Mahiou, Mitsunori Ono, Lijun Sun, Shoujun Chen, Shijie Zhang, Jun Jiang, Dinesh Chimmanamada, Chih-Yi Yu
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Publication number: 20140100226Abstract: The present invention provides a oxazole compound represented by Formula (1), or a salt thereof: wherein R1 is an aryl group which may have one or more substituents; R2 is an aryl group or a nitrogen atom-containing heterocyclic group each of which may have one or more substituents; and W is a divalent group represented by —Y1-A1- or —Y2—C(?O)— wherein Y1 is a group such as —C(?O)—, A1 is a group such as a lower alkylene group, and Y2 is a group such as a piperazinediyl group. The oxazole compound has a specific inhibitory action against phosphodiesterase 4.Type: ApplicationFiled: December 12, 2013Publication date: April 10, 2014Applicant: Otsuka Pharmaceutical Co., Ltd.Inventors: Minoru OKADA, Masaya KATO, Norifumi SATO, Tetsuyuki UNO, Hideki KITAGAKI, Junpei HARUTA, Hidetaka HIYAMA, Tomonori SHIBATA
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Patent number: 8691855Abstract: This present invention relates to novel compounds, isomer thereof or pharmaceutically acceptable salts thereof as vanilloid receptor (Vanilloid Receptor 1; VR1; TRPV1) antagonist; and a pharmaceutical composition containing the same. The present invention provides a pharmaceutical composition for preventing or treating a disease such as pain, migraine, arthralgia, neuralgia, neuropathies, nerve injury, skin disorder, urinary bladder hypersensitiveness, irritable bowel syndrome, fecal urgency, a respiratory disorder, irritation of skin, eye or mucous membrane, stomach-duodenal ulcer, inflammatory diseases, ear disease, heart disease and so on.Type: GrantFiled: July 2, 2009Date of Patent: April 8, 2014Assignee: Amorepacific CorporationInventors: Byoung Young Woo, Sun-Young Kim, Yeonjoon Kim, Song Seok Shin, Jin Kwan Kim, Ki-Wha Lee, Dong Hyun Kim, Kyung Min Lim, Joo-Hyun Moh, Yeon Su Jeong, Jin Kyu Choi, Hyun Ju Koh, Jeongho Lee, Hyuk Kim, Jeong Hoon Yoon, Funan Li, Jee-Suk Kim, Young-Ger Suh
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Publication number: 20140094474Abstract: Compounds of formula (I) or (II) wherein Rx, Rz, R9, R10, R14, R14?, R15, R15?, A and B are as defined in the claims and pharmaceutically acceptable salts and esters thereof, are disclosed. The compounds possess utility as tissue-selective androgen receptor modulators (SARM) and are useful as medicaments in the treatment of prostate cancer and other AR dependent conditions and diseases where AR antagonism is desired.Type: ApplicationFiled: April 20, 2012Publication date: April 3, 2014Applicant: ORION CORPORATIONInventors: Olli Törmakängas, Gerd Wohlfahrt, Harri Salo, Rathna Durga Ramasurbamanian, Pranab Kumar Patra, Arputharaj Ebenezer Martin, Terhi Heikkinen, Anniina Vesalainen, Anu Moilanen, Arja Karjalainen
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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: 8680100Abstract: The present invention is directed to compounds represented by structural formula (I), or a pharmaceutically acceptable salt or a transition metal chelate, coordinate or complex thereof or a transition metal chelate, coordinate or complex of a deprotonated form of the compound. Pharmaceutical composition and method of use for these compounds are also included.Type: GrantFiled: December 1, 2009Date of Patent: March 25, 2014Assignee: Synta Pharmaceuticals Corp.Inventors: Jun Jiang, Teresa Kowalczyk-Przewloka, Stefan M. Schweizer, Zhi-Qiang Xia, Shoujun Chen, Christopher Borella, Lijun Sun
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Patent number: 8680127Abstract: The present invention relates to N-cycloalkyl-N-biphenylmethyl-carboxamide derivatives of formula (I) wherein A, Z1, Z2, Z3, X, n, Y and m represent various substituents, their process of preparation, preparation intermediate compounds, their use as fungicide active agents, particularly in the form of fungicide compositions and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.Type: GrantFiled: July 30, 2009Date of Patent: March 25, 2014Assignee: Bayer Intellectual Property GmbHInventors: Philippe Desbordes, Ralf Dunkel, Stephanie Gary, Marie-Claire Grosjean-Cournoyer, Benoit Hartmann, Philippe Rinolfi, Jean-Pierre Vors, Rachel Rama
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Patent number: 8673911Abstract: This invention relates to compounds and methods for the inhibition of HDAC enzymatic activity. More particularly, the invention provides for compounds of formula (I), (I) and N-oxides, hydrates, solvates, pharmaceutically acceptable salts, prodrugs and complexes thereof, and racemic and scalemic mixtures, diastereomers and enantiomers thereof, wherein L, M, n, R, W, X and Y are as defined in the specification.Type: GrantFiled: November 3, 2008Date of Patent: March 18, 2014Assignee: MethylGene Inc.Inventors: Tammy Mallais, Oscar Moradei, Alain Ajamian, Pierre Tessier, David Smil, Sylvie Frechette, Silvana Leit, Patrick Beaulieu, Robert Deziel, John Mancuso
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Publication number: 20140073622Abstract: To develop an antibiotic having a novel mechanism of action, the present inventors have searched for a compound that has weak cytotoxicity, the physical property of high solubility in water, the effect of inhibiting both DNA gyrase GyrB and topoisomerase IV ParE subunits, and sufficient antibacterial activity. As a result, the present inventors have completed the present invention by finding that a compound of the present invention represented by the general formula (1), a pharmacologically acceptable salt thereof, and a prodrug thereof have desirable properties. The present invention provides a pharmaceutical composition (particularly, a preventive or therapeutic composition for infectious disease) comprising a compound represented by the formula (1), a pharmacologically acceptable salt thereof, or a prodrug thereof as an active ingredient.Type: ApplicationFiled: September 13, 2013Publication date: March 13, 2014Applicant: Daiichi Sankyo Company, LimitedInventors: Tsuyoshi Soneda, Hiroshi Takeshita, Yoshiko Kagoshima, Yuko Yamamoto, Takafumi Hosokawa, Toshiyuki Konosu, Nobuhisa Masuda, Takuya Uchida, Issei Achiwa, Junichi Kuroyanagi, Tetsunori Fujisawa, Aki Yokomizo, Tetsuji Noguchi
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Publication number: 20140066425Abstract: Disclosed are substituted thioimidazolidinone compounds and pharmaceutical compositions comprising such compounds. The compounds and compositions can be used for treatment of androgen receptor-associated diseases or disorders, such as prostate cancer, benign prostatic hypertrophy, male hair loss and hypertrichosis.Type: ApplicationFiled: March 8, 2012Publication date: March 6, 2014Applicants: SUZHOU KINTOR PHARMACEUTICALS, INC.Inventor: Youzhi Tong
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Publication number: 20140066420Abstract: The present invention relates to wherein each symbol is as defined in the specification. The compound of the present invention has a superior RBP4-lowering action, and is useful as a medicament for the prophylaxis or treatment of disease and condition mediated by increased RBP4.Type: ApplicationFiled: October 16, 2013Publication date: March 6, 2014Applicant: Takeda Pharmaceutical Company LimitedInventors: Shizuo KASAI, Tomohiro KAKU, Masahiro KAMAURA
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Publication number: 20140051680Abstract: This invention relates to generally inhibiting histone deacetylase (HDAC) enzymes (e.g., HDAC1, HDAC2, and HDAC3).Type: ApplicationFiled: February 28, 2012Publication date: February 20, 2014Applicant: REPLIGEN CORPORATIONInventors: Vincent Jacques, James R. Rusche, Norton P. Peet, Jasbir Singh
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Patent number: 8653118Abstract: The present invention provides compounds, that are N-alkyl-2-(1-(5-substituted-2-(3-oxo-3-(trifluoromethylsulfon-amido)propyl)benzyl)pyrrolidin-2-yl)oxazole-4-carboxamide wherein the 5 substituent is selected from the group consisting of halo and alkyloxy radicals. The compound may be represented by the following formula wherein R1 is selected from the group consisting of CO2R7 and CON(R7)SO2R7 wherein R1, R2, R3, R4, and R7 are as defined in the specification. The compounds may be administered to treat DP1, FP, EP1, EP3, TP and/or EP4 receptor mediated diseases or conditions.Type: GrantFiled: August 19, 2011Date of Patent: February 18, 2014Assignee: Allergan, Inc.Inventors: Jose L. Martos, William R. Carling, David F. Woodward, Jenny W. Wang, Jussi J Kangasmetsa
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Patent number: 8653070Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: GrantFiled: December 14, 2010Date of Patent: February 18, 2014Assignee: Enanta Pharmaceuticals, Inc.Inventors: Yao-Ling Qiu, Ce Wang, Xiaowen Peng, Hui Cao, Lu Ying, Yat Sun Or
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Patent number: 8653062Abstract: The present invention relates to novel cyclic amine and cycloalkyl derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.Type: GrantFiled: November 22, 2010Date of Patent: February 18, 2014Assignee: Allergan, Inc.Inventors: Phong X. Nguyen, Todd M. Heidelbaugh
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Publication number: 20140039009Abstract: The invention relates to compounds of structural formulas (I), (VII) and (XI): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein X1, X2, X3, Y, Z, L, R1, R2, R3, R18 and n are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.Type: ApplicationFiled: October 15, 2013Publication date: February 6, 2014Applicant: Synta Pharmaceuticals Corp.Inventors: Lijun Sun, Shoujun Chen, Zhiqiang Xia, Jun Jiang, Yu Xie, Junyi Zhang
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Patent number: 8637559Abstract: The present invention provides a oxazole compound represented by Formula (1), or a salt thereof: wherein R1 is an aryl group which may have one or more substituents; R2 is an aryl group or a nitrogen atom-containing heterocyclic group each of which may have one or more substituents; and W is a divalent group represented by —Y1-A1- or —Y2—C(?O)— wherein Y1 is a group such as —C(?O)—, A1 is a group such as a lower alkylene group, and Y2 is a group such as a piperazinediyl group. The oxazole compound has a specific inhibitory action against phosphodiesterase 4.Type: GrantFiled: November 14, 2006Date of Patent: January 28, 2014Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Minoru Okada, Masaya Kato, Norifumi Sato, Tetsuyuki Uno, Hideki Kitagaki, Junpei Haruta, Hidetaka Hiyama, Tomonori Shibata
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Patent number: 8633182Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, R2, R3, m and n are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2. Furthermore, the invention relates to novel intermediates, useful for the synthesis of compounds of formula I.Type: GrantFiled: May 22, 2013Date of Patent: January 21, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Dieter Hamprecht, Sara Frattini, Iain Lingard, Stefan Peters
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Publication number: 20140018389Abstract: This disclosure concerns novel compounds of Formula (I) or as defined in the specification and compositions comprising such novel compounds. These compounds are useful antiviral agents, especially in inhibiting the function of the NS5A protein encoded by Hepatitis C virus (HCV). Thus, the disclosure also concerns a method of treating HCV related diseases or conditions by use of these novel compounds or a composition comprising such novel compounds.Type: ApplicationFiled: September 16, 2013Publication date: January 16, 2014Inventors: Rico Lavoie, John A. Bender, Jeffrey Lee Romine, Edward H. Ruediger, Carol Bachand, Omar D. Lopez, Qi Chen, Makonen Belema, John F. Kadow, Lawrence G. Hamann
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Publication number: 20140011997Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.Type: ApplicationFiled: September 12, 2013Publication date: January 9, 2014Applicant: THERAVANCE, INC.Inventors: Cameron Smith, Melissa Fleury, Roland Gendron, Ryan Hudson, Adam D. Hughes
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Patent number: 8623860Abstract: The invention relates to new azetidine derivatives of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.Type: GrantFiled: December 14, 2012Date of Patent: January 7, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Martin Fleck, Bernd Nosse, Gerald Juergen Roth
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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: 20130324579Abstract: The present invention relates to pyrazole and imidazole derivatives of formula (I) wherein U, V, L, X, Y, R1, (R2)n and (R3)m and ring A are as described in the description, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), and especially to their use as orexin receptor antagonists.Type: ApplicationFiled: February 17, 2012Publication date: December 5, 2013Applicant: ACTELION PHARMACEUTICALS LTD.Inventors: Martin Bolli, Christoph Boss, Christine Brotschi, Markus Gude, Bibia Heidmann, Thierry Sifferlen, Jodi T. Williams
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Patent number: 8598365Abstract: Bicyclic dione compounds, and derivatives thereof, which are suitable for use as herbicides.Type: GrantFiled: July 30, 2008Date of Patent: December 3, 2013Assignee: Syngenta LimitedInventors: Stephane André Marie Jeanmart, Christopher John Mathews, John Benjamin Taylor, Steve Smith
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Publication number: 20130310427Abstract: Antiviral compounds may be used to inhibit or reduce the activity of Hepatitis C virus (HCV), particularly HCV's NS5A protein. In these contexts, inhibition and reduction of activity of the NS5A protein refers to a lower level of the measured activity relative to a control experiment in which the cells or the subjects are not treated with the test compound. The inhibition or reduction in the measured activity is at least a 10% reduction or inhibition. The compounds and their isomeric forms and pharmaceutically acceptable salts thereof are useful in treating and preventing HCV infection alone or when used in combination with other compounds targeting viral or cellular elements or functions involved in the HCV lifecycle.Type: ApplicationFiled: June 9, 2011Publication date: November 21, 2013Applicant: PRESIDIO PHARMACEUTICALS, INC.Inventors: Leping Li, Min Zhong
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Patent number: 8586571Abstract: The present invention relates to wherein each symbol is as defined in the specification. The compound of the present invention has a superior RBP4-lowering action, and is useful as a medicament for the prophylaxis or treatment of disease and condition mediated by increased RBP4.Type: GrantFiled: October 17, 2008Date of Patent: November 19, 2013Assignee: Takeda Pharmaceutical Company LimitedInventors: Shizuo Kasai, Tomohiro Kaku, Masahiro Kamaura
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Publication number: 20130296310Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is a group of formula A or formula B, and X, R2, R3, R4, R5, R6, Ra and Rb are as defined herein. Also provided are methods of using the compounds for treating diseases mediated by a P2X3 and/or a P2X2/3 receptor antagonist and methods of making the subject compounds.Type: ApplicationFiled: July 1, 2013Publication date: November 7, 2013Inventors: Li Chen, Michael Patrick Dillon, Lichun Feng, Ronald Charles Hawley, Minmin Yang
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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: 20130267569Abstract: The invention relates to hydroxylated aminotriazole derivatives of formula (I), wherein Q, R1, R2, R3 and R4 are as defined in the description, their preparation and their use as pharmaceutically active compounds.Type: ApplicationFiled: December 6, 2011Publication date: October 10, 2013Inventors: Daniel Bur, Olivier Corminboeuf, Sylvaine Cren, Corinna Grisostomi, Xavier Leroy, Sylvia Richard-Bildstein
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Patent number: 8552039Abstract: The present invention relates to novel compounds, methods, and formulations useful for the oral delivery of a GLP-1 compound or an MC4 agonist peptide.Type: GrantFiled: December 11, 2009Date of Patent: October 8, 2013Assignee: Emisphere Technologies, Inc.Inventors: Robert Jason Herr, Louis Nickolaus Jungheim, John McNeil McGill, Kenneth Jeff Thrasher, Muralikrishna Valluri
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Patent number: 8552003Abstract: The present invention is directed to a compound of the formula: or pharmaceutically acceptable salts thereof and use of such compounds for treating proliferative diseases such as cancer, in mammals.Type: GrantFiled: July 31, 2007Date of Patent: October 8, 2013Assignee: Novartis AGInventors: Mark G. Charest, Christine Hiu-Tung Chen, Zhuoliang Chen, Miao Dai, Feng He, Huangshu Lei, Ly Luu Pham, Sushil Kumar Sharma, Christopher Sean Straub, Run-Ming David Wang, Fan Yang, Leigh Zawel
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Publication number: 20130261159Abstract: The invention relates to oxazolyl-methylether derivatives of formula (I), wherein R1, R2, R3, R4 and R5 are as defined in the description, their preparation and their use as pharmaceutically active compounds.Type: ApplicationFiled: December 6, 2011Publication date: October 3, 2013Applicant: Actelion Pharmaceuticals Ltd.Inventors: Daniel Bur, Olivier Corminboeuf, Sylvaine Cren, Corinna Grisostomi, Xavier Leroy, Sylvia Richard-Bildstein
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Patent number: 8546336Abstract: The present invention is directed to a compound of the formula: or pharmaceutically acceptable salts thereof and use of such compounds for treating proliferative diseases such as cancer, in mammals.Type: GrantFiled: September 7, 2012Date of Patent: October 1, 2013Assignee: Novartis AGInventors: Zhuoliang Chen, Mark G. Charest, Christine Hiu-Tung Chen, Miao Dai, Feng He, Huangshu Lei, Ly Luu Pham, Sushil Kumar Sharma, Christopher Sean Straub, Run-Ming David Wang, Fan Yang, Leigh Zawel
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Patent number: 8546400Abstract: Oxazole derivatives are described. The inventive compounds are useful as kinase inhibitors, and may be used in the treatment of cancer, such as prostate cancer, lung cancer, breast cancer, colon cancer, leukemia, CNS cancer, melanoma, ovarian cancer, and renal cancer.Type: GrantFiled: January 9, 2013Date of Patent: October 1, 2013Assignee: Neosome Life Sciences, LLCInventors: Laxman S. Desai, Srinivas Chittaboina
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Patent number: 8541594Abstract: Bicyclic dione compounds, and derivatives thereof, which are suitable for use as herbicides.Type: GrantFiled: July 30, 2008Date of Patent: September 24, 2013Assignee: Syngenta LimitedInventors: Stephane André Marie Jeanmart, Christopher John Mathews, John Benjamin Taylor, Steve Smith
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Patent number: 8530460Abstract: Azetidine derivatives of which the following is exemplary and their use in the treatment of obesity, diabetes or dyslipidemia.Type: GrantFiled: December 14, 2012Date of Patent: September 10, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Martin Fleck, Bernd Nosse, Niklas Heine, Gerald Juergen Roth