Additional Hetero Ring Which Is Unsaturated Patents (Class 544/333)
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Publication number: 20140155381Abstract: The present invention relates to novel retinoid-related orphan receptor gamma (ROR?) modulators and their use in the treatment of diseases mediated by ROR?.Type: ApplicationFiled: July 27, 2012Publication date: June 5, 2014Inventors: Erkan Baloglu, Gary J. Bohnert, Shomir Ghosh, Mercedes Lobera, Darby R. Schmidt, Leonard Sung
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Publication number: 20140155597Abstract: The purpose of the present invention is to provide a novel compound which has an anti-fungal activity on pathogenic fungi including fungi belonging to the genus Candida, the genus Aspergillus and the genus Trichophyton and is useful as a medicinal agent.Type: ApplicationFiled: July 27, 2012Publication date: June 5, 2014Applicants: TOYAMA CHEMICAL CO., LTD., TAISHO PHARMACEUTICAL CO., LTD.Inventors: Tetsuya Tanikawa, Yasunobu Ushiki, Fumihito Ushiyama, Toru Yamaguchi, Naoya Ono, Keiko Yamamoto, Risa Tsuruta, Yasuhiro Tsutsui, Noritomo Fujino, Ayumu Mori
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Publication number: 20140155407Abstract: The present invention relates to compounds which selectively inhibit CYP11B1. Preferably, the compounds of the present invention do not substantially inhibit CYP11B2. Moreover, the compounds of the present invention do not substantially inhibit CYP17 and/or CYP19, either. Amongst other applications of the compounds of the present invention, they can be used for the treatment of Cushing's syndrome or metabolic disease.Type: ApplicationFiled: October 21, 2011Publication date: June 5, 2014Inventors: Rolf Hartmann, Ulrike Hille, Christina Zimmer, Carsten A. Vock, Qingzhong Hu
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Patent number: 8741450Abstract: A material for organic electroluminescence devices comprising a compound in which a heterocyclic group having nitrogen is bonded to an arylcarbazolyl group or a carbazolylalkylene group and an organic electroluminescence device comprising an anode, a cathode and an organic thin film layer comprising at least one layer and disposed between the anode and the cathode, wherein at least one layer in the organic thin film layer comprises the material for organic electroluminescence devices described above. The material can provide an organic electroluminescence device emitting bluish light with a high purity of color. The organic electroluminescence device uses the material.Type: GrantFiled: August 31, 2012Date of Patent: June 3, 2014Assignee: Idemitsu Kosan Co., Ltd.Inventors: Toshihiro Iwakuma, Hiroshi Yamamoto, Yoshio Hironaka, Hidetsugu Ikeda, Chishio Hosokawa, Seiji Tomita, Takashi Arakane
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Patent number: 8742106Abstract: The invention relates to compound of the formula (I?) in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it.Type: GrantFiled: December 20, 2010Date of Patent: June 3, 2014Assignee: Novartis AGInventors: Sangamesh Badiger, Dirk Behnke, Claudia Betschart, Vinod Chaudhari, Murali Chebrolu, Simona Cotesta, Samuel Hintermann, Arndt Meyer, Chetan Pandit
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Patent number: 8741897Abstract: Compounds of Formula (IA), (IB), (IC), and (ID) wherein R1, R2, R3, R4, R5, and R6 are as respectively defined herein for Formula (IA), (IB), (IC), and (ID), or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.Type: GrantFiled: September 22, 2004Date of Patent: June 3, 2014Assignee: Boehringer Ingelheim Pharmaceuticals Inc.Inventors: Younes Bekkali, Rajashekhar Betageri, Michel J. Emmanuel, Abdelhakim Hammach, Christian Hanke Justus Joachim Harcken, Thomas Martin Kirrane, Jr., Daniel Kuzmich, Thomas Wai-Ho Lee, Pingrong Liu, Usha R. Patel, John Robert Proudfoot, Hossein Razavi, Doris Riether, Hidenori Takahashi, David S. Thomson, Ji Wang, Renee Zindell
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Patent number: 8741892Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, X, R1, R2, R3 have meanings given in the description.Type: GrantFiled: November 30, 2012Date of Patent: June 3, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Matthias Grauert, Daniel Bischoff, Georg Dahmann, Raimund Kuelzer, Klaus Rudolf, Bernd Wellenzohn
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Publication number: 20140148453Abstract: Disclosed are sulfonamide compounds of Formula (I): or stereoisomers, N-oxides, prodrugs, or pharmaceutically acceptable salts thereof, wherein ring A, R1, R2, R3, R4 and R5 are defined herein. Also disclosed are methods of using such compounds in the treatment of conditions related to CYP17 enzyme, such as cancer, and pharmaceutical compositions comprising such compounds.Type: ApplicationFiled: July 25, 2011Publication date: May 29, 2014Inventors: Joel Francis Austin, Lisa S. Sharma, James Aaron Balog, Audris Huang, Upender Velaparthi, Chetan Padmakar Darne, Mark George Saulnier
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Publication number: 20140142108Abstract: This invention provides compounds of formula (I): wherein R1a, R1b, R1c, R1d, R2a, R2b, X1, X2, and G have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.Type: ApplicationFiled: May 30, 2013Publication date: May 22, 2014Inventors: Christopher Blackburn, Kenneth M. Gigstad, He Xu
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Publication number: 20140142085Abstract: The invention provides compounds of formula (I): or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula (I), processes for preparing compounds of formula (I), intermediates useful for preparing compounds of formula I and therapeutic methods for treating a Retroviridae viral infection including an infection caused by the HIV virus.Type: ApplicationFiled: July 5, 2012Publication date: May 22, 2014Applicant: Gilead Sciences, Inc.Inventors: Steven S. Bondy, Carina E. Cannizzaro, Chien-hung Chou, Randall L. Halcomb, Yunfeng Eric Hu, John O. Link, Qi Liu, Scott D. Schroeder, Winston C. Tse, Jennifer R. Zhang
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Patent number: 8729091Abstract: This invention relates to novel phenyl amide or pyridyl amide derivatives of the formula wherein A1, A2, B1, B2 and R1 to R11 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are GPBAR1 agonists and can be used as medicaments for the treatment of diseases such as type II diabetes.Type: GrantFiled: February 15, 2013Date of Patent: May 20, 2014Assignee: Hoffmann-La Roche Inc.Inventors: Caterina Bissantz, Henrietta Dehmlow, Shawn David Erickson, Kyungjin Kim, Rainer E. Martin, Ulrike Obst Sander, Sherrie Lynn Pietranico-Cole, Hans Richter, Christoph Ullmer
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Publication number: 20140135333Abstract: 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: January 16, 2014Publication date: May 15, 2014Applicant: THERAVANCE, INC.Inventors: Paul R. Fatheree, Robert Murray McKinnell
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Publication number: 20140135332Abstract: The present invention provides compounds of Formula (I): and salts, racemates, isomers, diastereoisomers, enantiomers, hydrates, solvates, N-oxides, pharmaceutically acceptable derivatives or prodrugs thereof. Also provided the use of these compounds as antibacterials, compositions comprising them and processes for their manufacture.Type: ApplicationFiled: April 20, 2012Publication date: May 15, 2014Applicant: BIOTA SCIENTIFIC MANAGEMENT PTY LTDInventors: David John Haydon, Lloyd George Czaplewski, Neil Robert Stokes, David Davies, Ian Collins, James T Palmer, Jeffrey Peter Mitchell, Gary Robert William Pitt, Daniel Offermann
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Publication number: 20140135346Abstract: The present application relates to novel amides and thioamides, to processes for preparation thereof and to the use thereof for controlling animal pests, in particular arthropods and especially insects.Type: ApplicationFiled: January 16, 2014Publication date: May 15, 2014Applicant: Bayer CropScience AGInventors: Thomas BRETSCHNEIDER, Adeline KÖHLER, Reiner FISCHER, Martin FÜßLEIN, Peter JESCHKE, Joachim KLUTH, Friedrich August MÜHLTHAU, Arnd VOERSTE, Olga MALSAM, Ulrich GÖRGENS, Yoshitaka SATO
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Publication number: 20140135328Abstract: The present invention relates to compounds of the formula I, wherein A, D, E, L, G, R10, R30, R40, R50 and R60 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin A, and are useful for the treatment of diseases such as atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.Type: ApplicationFiled: January 17, 2014Publication date: May 15, 2014Applicant: SANOFIInventors: Sven Ruf, Thorsten Sadowski, Klaus Wirth, Herman Schreuder, Christian Buning
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Patent number: 8722687Abstract: The invention relates to new bicyclic heterocyclyl derivatives of formula (I), to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.Type: GrantFiled: April 15, 2010Date of Patent: May 13, 2014Assignee: Astex Therapeutics LtdInventors: Gordon Saxty, Valerio Berdini, Christopher William Murray, Eddy Jean Edgard Freyne, Yannick Aimé Eddy Ligny, Pascal Ghislain André Bonnet, Berthold Wroblowski, Alexandra Papanikos
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Patent number: 8722678Abstract: Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, wherein E, X, G, W2 and Z 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. Also disclosed are compounds of Formula 1A including all stereoisomers, N-oxides, and salts thereof, wherein E, X, G and Z1 are as defined in the disclosure. Also disclosed is the use of the compounds of Formula 1A as intermediates for preparing compounds of Formula 1.Type: GrantFiled: April 15, 2011Date of Patent: May 13, 2014Assignee: E I du Pont de Nemours and CompanyInventors: Mary Ann Hanagan, Eric Allen Marshall
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Patent number: 8722905Abstract: Disclosed is a dye, having a chemical formula: wherein each R1 is independently selected from hydrogen, —(CxH2x+1), —(CyH2y)—S—(CxH2x+1), or —(CyH2y)—N(CxH2x+1)2; Ar1 is wherein each R2 is independently selected from —(CxH2x+1), —(CxH2x)—S—(CxH2x+1), or (CxH2x)—N(CxH2x+1)2; Ar2 is wherein each R3 is independently selected from hydrogen, —(CxH2x+1), —(CyH2y)—S—(CxH2x+1), or —(CyH2y)—N(CxH2x+1)2; X is sulfur, oxygen, selenium, or N—R4, and R4 is —(CxH2x+1); m is in integer of 1 to 4; x is an integer of 1 to 20; and y is an integer of 0 to 20. The dye can be applied to a photoelectric conversion device.Type: GrantFiled: August 3, 2012Date of Patent: May 13, 2014Assignee: Industrial Technology Research InstituteInventors: Yao-Shan Wu, Yung-Liang Tung, Jen-An Chen, Chun-Guey Wu, Jheng-Ying Li
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Publication number: 20140128374Abstract: The present invention provides, in part, compounds of Formula I: and pharmaceutically acceptable salts thereof and N-oxides of the foregoing; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds, salts or N-oxides, and their uses for treating D1-mediated (or D1-associated) disorders including, e.g., schizophrenia (e.g., its cognitive and negative symptoms), cognitive impairment (e.g., cognitive impairment associated with schizophrenia, AD, PD, or pharmacotherapy therapy), ADHD, impulsivity, compulsive gambling, overeating, autism spectrum disorder, MCI, age-related cognitive decline, dementia, RLS, Parkinson's disease, Huntington's chorea, anxiety, depression, MDD, TRD, and bipolar disorder.Type: ApplicationFiled: November 5, 2013Publication date: May 8, 2014Applicant: PFIZER INCInventors: JENNIFER ELIZABETH DAVOREN, AMY BETH DOUNAY, IVAN VIKTOROVICH EFREMOV, DAVID LAWRENCE FIRMAN GRAY, SCOT RICHARD MENTE, STEVEN VICTOR O'NEIL, BRUCE NELSEN ROGERS, CHAKRAPANI SUBRAMANYAM, LEI ZHANG
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Publication number: 20140128406Abstract: The present invention relates to heterocyclic compounds of formula I which have microbiocidal activity, in particular fungicidal activity as well as methods of using the compounds of formula (I) to control microbes: wherein A is x-C(R10R11)—C(?O)—, x-C(R12R13)—C(?S)—, x-O—C(?O)—, x-O—C(?S)—, x-N(R14)—C(?O)—, x-N(R15)—C(?S)—, x-C(R16R17)—SO2— or x-N?C(R30)—, in each case x indicates the bond that is connected to R1; T is CR18 or N; Y1, Y2, Y3, and Y4 are independently CR19 or N; Q is O or S; n is 1 or 2; p is 1 or 2, providing that when n is 2, p is 1.Type: ApplicationFiled: June 27, 2012Publication date: May 8, 2014Applicant: SYNGENTA PARTICIPATIONS AGInventors: Sarah Sulzer-Mosse, Clemens Lamberth, Fredrik Emil Malcolm Cederbaum
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Publication number: 20140128367Abstract: The invention provides certain cycloalkyl-fused tetrahydroquinolines of the Formula (I), and their pharmaceutically acceptable salts and esters, wherein R1, R2, R7, R8a, E, Y, Z, n, u, and t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions associated with uncontrolled or inappropriate stimulation of CRTH2 function.Type: ApplicationFiled: June 14, 2012Publication date: May 8, 2014Applicant: Merck Sharp & Dohme Corp.Inventors: Xianhai Huang, Jason Brubaker, Scott L. Peterson, John W. Butcher, Joshua T. Close, Michelle Martinez, Rachel Nicola MacCoss, Joon O. Jung, Phieng Siliphaivanh, Hongjun Zhang, Robert G. Aslanian, Purakkattle Johny Biju, Li Dong, Ying Huang, Kevin D. McCormick, Anandan Palani, Ning Shao, Wei Zhou
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Publication number: 20140128363Abstract: The present invention is directed to a new class of hydroxamic acid derivatives, their use as LpxC inhibitors, and more specifically their use to treat bacterial infections.Type: ApplicationFiled: January 14, 2014Publication date: May 8, 2014Inventors: Matthew Frank Brown, Ye Che, Anthony Marfat, Michael Joseph Melnick, Justin Ian Montgomery, Usa Reilly
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Publication number: 20140128373Abstract: Compounds active on protein kinases are described, as well as methods of making and using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.Type: ApplicationFiled: February 1, 2012Publication date: May 8, 2014Inventors: Prabha N. Ibrahim, Chao Zhang, Wayne Spevak, Jiazhong Zhang, Guoxian Wu, Jack Lin, Hanna Cho, Marika Nespi, Songyuan Shi, Todd Ewing, Ying Zhang
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Patent number: 8716292Abstract: The present invention relates to riminophenazines having heteroaromatic substitutions, including those with 2-heteroaryl-amino substituents, to their preparation, and to their use as drugs for treating Mycobacterium tuberculosis and other microbial infections, either alone or in combination with other anti-infective treatments. A general representation of the 2-(heteroaryl)amino-riminophenazines is shown below.Type: GrantFiled: June 28, 2011Date of Patent: May 6, 2014Assignee: Global Alliance for TB Drug DevelopmentInventors: Kai Liu, Christopher B. Cooper, Haihong Huang, Chun Li, Binna Liu, Yang Liu, Zhenkun Ma, Jingbin Wang, Dali Yin, Dongfeng Zhang, Gang Zhang, Hao Zhang
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Patent number: 8710055Abstract: The present invention encompasses compounds of general formula (I) wherein the groups R2 to R4, A, X and m are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, pharmaceutical preparations which contain compounds of this kind and their use as medicaments.Type: GrantFiled: December 19, 2011Date of Patent: April 29, 2014Assignee: Boehringer Ingelheim International GmbHInventor: Steffen Steurer
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Publication number: 20140114068Abstract: Disclosed are novel indanone derivatives, pharmaceutically acceptable salts thereof or enantiomers, a preparation method thereof, and a pharmaceutical composition for the prevention or treatment of viral diseases, comprising the same as an active ingredient. The indanone derivatives have excellent inhibitory activity against picornaviruses including coxsackie-, entero-, echo-, Polio-, and rhinoviruses, as well as exhibiting low cytotoxicity, so that they can be useful as an active ingredient of a pharmaceutical composition for the prevention or treatment of viral diseases including poliomyelitis, paralysis, acute hemorrhagic conjunctivitis, viral meningitis, hand-foot-and-mouth disease, vesicular disease, hepatitis A, myositis, myocarditis, pancreatitis, diabetes, epidemic myalgia, encephalitis, flu, herpangina, foot-and-mouth disease, asthma, chronic obstructive pulmonary disease, pneumonia, sinusitis or otitis media.Type: ApplicationFiled: June 18, 2012Publication date: April 24, 2014Applicants: KATHOLIEKE UNIVERSITEIT LEUVEN K.U. LEUVEN R & D, KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGYInventors: Young Sik Jung, Chong Kgo Lee, Hae Soo Kim, Hee Chun Jeong, Pil Ho Kim, Soo Bong Han, Jin Soo Shin, Johan Neyts, Hendrik Jan Thibaut
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Publication number: 20140113897Abstract: The present invention embraces compounds that modulate the activity of Epstein-Barr Nuclear Antigen 1 (BBNA1) protein and use thereof in methods for treating latent Epstein-Barr virus infection. R7 is a substituted or unsubstituted phenyl, pyridyl, or pyrimidinyl group. A pharmaceutical composition comprising a compound of the invention in admixture with a pharmaceutically acceptable carrier is also provide as are methods for modulating the activity of Epstein-Barr Nuclear Antigen 1 (EBNA1) protein and treating a latent EpsteinBarr virus infection with a composition of the present invention.Type: ApplicationFiled: May 22, 2012Publication date: April 24, 2014Applicant: THE WISTAR INSTITUTEInventors: Paul M. Lieberman, Troy Messick
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Publication number: 20140113907Abstract: The present invention provides a pyridylaminoacetic acid compound represented by the following formula (1): (wherein R1, R2, R3, Y and Z are as defined in the description and claims), or a pharmacologically acceptable salt thereof. Since the pyridylaminoacetic acid compound has EP2 agonistic action, it is useful as a therapeutic or prophylactic drug for respiratory diseases such as asthma or chronic obstructive pulmonary disease.Type: ApplicationFiled: December 16, 2013Publication date: April 24, 2014Applicant: UBE INDUSTRIES, LTD.Inventors: Ryo IWAMURA, Masayuki TANAKA, Tetsushi KATSUBE, Manabu SHIGETOMI, Eiji OKANARI, Yasunori TOKUNAGA, Hiroshi FUJIWARA
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Patent number: 8703759Abstract: The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein R1, R2, R3, R4, and R5 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.Type: GrantFiled: June 30, 2011Date of Patent: April 22, 2014Assignee: Gilead Sciences, Inc.Inventors: Tetsuya Kobayashi, Dmitry Koltun, Gregory Notte, Eric Parkhill, Jeff Zablocki
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Patent number: 8703103Abstract: Sterically hindered imidazole ligands are described, along with their synthesis, which are capable of coordinating to Group 2 metals, such as: calcium, magnesium, strontium, in an eta-5 coordination mode which permits the formation of monomeric or dimeric volatile complexes. A compound comprising one or more polysubstituted imidazolate anions coordinated to a metal selected from the group consisting of barium, strontium, magnesium, radium or calcium or mixtures thereof. Alternatively, one anion can be substituted with and a second non-imidazolate anion. Synthesis of the novel compounds and their use to form BST films is also contemplated.Type: GrantFiled: January 28, 2011Date of Patent: April 22, 2014Assignee: Air Products and Chemicals, Inc.Inventors: John Anthony Thomas Norman, Melanie K. Perez, Moo-Sung Kim
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Patent number: 8703781Abstract: A novel combination comprising the MEK inhibitor N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)6,8-dimethyl;-2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide, or a pharmaceutically acceptable salt or solvate thereof, with a B-Raf inhibitor, particularly N-{3-[5-(2-Amino-4-pyrimidinyl)-2-(1,1-dimethylethyl)-1,3-thiazol-4-yl]-2-fluorophen-}-2,6-difluorobenzenesulfonamide or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising the same and methods of using such combinations and compositions in the treatment of conditions in which the inhibition of MEK and/or B-Raf is beneficial, eg. cancer.Type: GrantFiled: October 15, 2010Date of Patent: April 22, 2014Assignee: GlaxoSmithKline LLCInventors: Melissa Dumble, Rakesh Kumar, Sylvie Laquerre, Peter Lebowitz
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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: 20140107340Abstract: The present invention is directed to benzamide containing compounds which inhibit the P2X7 receptorType: ApplicationFiled: October 10, 2013Publication date: April 17, 2014Applicant: H. Lundbeck A/SInventors: John Paul Kilburn, Lars Kyhn Rasmussen, Mikkel Jessing, Eman Mohammed Eldemenky, Bin Chen, Yu Jiang, Allen T. Hopper
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Publication number: 20140107097Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating ROR?t activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.Type: ApplicationFiled: October 15, 2013Publication date: April 17, 2014Applicant: Janssen Pharmaceutica NVInventors: Kristi A. Leonard, Kent Barbay, James P. Edwards, Kevin D. Kreutter, David A. Kummer, Umar Maharoof, Rachel Nishimura, Maud Urbanski, Hariharan Venkatesan, Aihua Wang, Ronald L. Wolin, Craig R. Woods, Anne Fourie, Xiaohua Xue, Taraneh Mirzadegan, Kelly Ganamet
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Patent number: 8697870Abstract: The present invention relates to 3-cycloalkylaminopyrrolidine derivatives of the formula I: (wherein R1, R2, R3, R4, R5, R6, R7, X, Y and Z are as defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of chemokine receptors and more specifically as modulators of the CCR2 and/or CCR5 receptor. The compounds and compositions of the invention may bind to chemokine receptors, e.g., the CCR2 and/or CCR5 chemokine receptors, and are useful for treating diseases associated with chemokine, e.g., CCR2 and/or CCR5, activity, such as atherosclerosis, restenosis, lupus, organ transplant rejection and rheumatoid arthritis.Type: GrantFiled: November 19, 2008Date of Patent: April 15, 2014Assignee: Incyte CorporationInventors: Chu-Biao Xue, Brian W. Metcalf, Amy Qi Han, Darius J. Robinson, Changsheng Zheng, Anlai Wang, Yingxin Zhang
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Patent number: 8697744Abstract: The present invention relates to novel compounds of Formula (I), wherein X1, X2, Y, Z1, Z2, Z3, M and (A)m are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors—subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.Type: GrantFiled: January 12, 2010Date of Patent: April 15, 2014Assignee: Addex Pharma S.A.Inventors: Christelle Boléa, Sylvain Celanire
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Publication number: 20140100108Abstract: 3-Phenylisoxazoline-5-carboxamides and 3-phenylisoxazoline-5-thioamides of the formula (I) and their use as herbicides and fungicides are described. In this formula (I), X, X2 to X6, R1 to R4 are radicals such as hydrogen, halogen and organic radicals such as substituted alkyl. A is a bond or a divalent unit. Y is a chalcogen.Type: ApplicationFiled: March 26, 2012Publication date: April 10, 2014Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Lothar Willms, Monika H. Schmitt, Thomas Frenzel, Klaus Bernhard Haaf, Isolde Haeuser-Hahn, Ines Heinemann, Elmar Gatzweiler, Christopher Hugh Rosinger, Jan Dittgen, Dieter Feucht, Jeffrey Martin Hills, Philippe Rinolfi, Heinz KEHNE
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Publication number: 20140100214Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including P13 kinase activity, are described herein.Type: ApplicationFiled: December 6, 2013Publication date: April 10, 2014Applicant: Infinity Pharmaceuticals, Inc.Inventors: Alfredo C. CASTRO, Catherine A. Evans, Somarajannair Janardanannair, Andre Lescarbeau, Tao Liu, Daniel A. Snyder, Martin R. Tremblay, Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan
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Publication number: 20140093505Abstract: The present invention relates to a pyridonaphthyridine compound as represented by general formula (I), which has a dual PI3K and mTOR inhibition effect, and its pharmaceutically acceptable salt, stereoisomer and deuteride thereof, wherein R1, R2, R3, R4, R5, R6, R7 and X are as defined in the specification; the present invention also relates to a method for preparing said compound, a pharmaceutical composition and a pharmaceutical formulation containing said compound, and uses of said compound in treating and/or preventing a proliferative disease and in the manufacture of a medicament for treating and/or preventing a proliferative disease.Type: ApplicationFiled: June 4, 2012Publication date: April 3, 2014Applicant: Xuanzhu Pharma Co., Ltd.Inventors: Frank Wu, Yan Zhang
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Patent number: 8685969Abstract: Compounds having formula (I), and enantiomers, and diastereomers, stereoisomers, pharmaceutically-acceptable salts thereof, formula (I) are useful as kinase modulators, including Btk modulation.Type: GrantFiled: June 16, 2011Date of Patent: April 1, 2014Assignee: Bristol-Myers Squibb CompanyInventors: Chunjian Liu, James Lin, George V. DeLucca, Douglas G. Batt, Qingjie Liu
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Patent number: 8686156Abstract: The present application relates to novel heterocyclic compounds, to their use for controlling animal pests including arthropods and in particular insects, and to processes for preparing the novel compounds.Type: GrantFiled: May 3, 2011Date of Patent: April 1, 2014Assignee: Bayer CropScience AGInventors: Martin Füβlein, Thomas Bretschneider, Reiner Fischer, Peter Jeschke, Adeline Köhler, Joachim Kluth, Friedrich August Mühlthau, Arnd Voerste, Yoshitaka Sato
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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
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Patent number: 8685986Abstract: The present invention is to provide a medical composition for the treatment or prophylaxis of glaucoma which comprises a pyridylaminoacetic acid compound represented by the formula (1): wherein R1, R2, R3, Y, and Z are defined in the specification.Type: GrantFiled: March 30, 2010Date of Patent: April 1, 2014Assignee: Ube Industries, Ltd.Inventors: Masahiko Hagihara, Kenji Yoneda, Eiji Okanari, Manabu Shigetomi
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Publication number: 20140088071Abstract: Compounds of Formula (IA) and Formula (IB) are described. They are useful as stimulators of sGC, particularly NO-independent, heme-dependent stimulators. These compounds may be useful for treating, preventing or managing various disorders that are herein disclosed.Type: ApplicationFiled: November 2, 2011Publication date: March 27, 2014Applicant: Ironwood Pharmaceuticals, Inc.Inventors: Takashi Nakai, Thomas Wai-Ho Lee, Charles Kim, Joel Moore, Nicholas Robert Perl, Jason Rohde
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Publication number: 20140088117Abstract: Cyclic ether pyrazol-4-yl-heterocyclyl-carboxamide compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein R2 is a cyclic ether and X is thiazolyl, pyrazinyl, pyridinyl, or pyrimidinyl, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: ApplicationFiled: September 25, 2013Publication date: March 27, 2014Applicant: Genentech, Inc.Inventors: Jason Burch, Minghua Sun, Xiaojing Wang, Wesley Blackaby, Alastair James Hodges, Andrew Sharpe
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Publication number: 20140088118Abstract: The present invention provides a compound useful as an agent for the prophylaxis or treatment of neurodegenerative disease and the like, or a salt thereof. The present invention relates to a compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.Type: ApplicationFiled: July 17, 2013Publication date: March 27, 2014Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Tatsuki KOIKE, Masato YOSHIKAWA, Haruhi KAMISAKI, William John FARNABY
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Publication number: 20140088305Abstract: The present invention relates to organic electroluminescent devices which comprise heteroaromatic compounds.Type: ApplicationFiled: May 7, 2012Publication date: March 27, 2014Applicant: Merck Patent GmbHInventors: Amir Hossain Parham, Arne Buesing, Christof Pflumm, Teresa Mujica-Fernaud, Philipp Toessel, Thomas Eberle
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Publication number: 20140088080Abstract: [Problem] An excellent drug for treating or preventing cardiovascular diseases, based on cGMP production enhancing action due to soluble guanylate cyclase activating action, is provided. [Means for Solution] It was found that imidazopyridine compounds having a carbamoyl group at the 3-position and a substituent bonded at the 8-position via an oxygen atom in an imidazo[1,2-a]pyridine skeleton exhibits a cGMP production enhancing action by a potent soluble guanylate cyclase activating action, and is useful as a drug for treating or preventing various soluble guanylate cyclase-related cardiovascular diseases, thereby completing the present invention.Type: ApplicationFiled: November 26, 2013Publication date: March 27, 2014Applicant: ASTELLAS PHARMA INC.Inventors: Yuji KOGA, Kyoichi MAENO, Ippei SATO, Yoshimasa IMAMURA, Takeshi HANAZAWA, Maiko IIDA, Kazuhiko OHNE, Kenichiro IMAMURA, Tsubasa WATANABE, Eisuke NOZAWA, Hiroshi SHIBATA
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4-phenyl-pyrane-3,5-diones,4-phenyl-thiopyrane-3,6-diones and cyclohexanetriones as novel herbicides
Patent number: 8680012Abstract: Pyrandione, thiopyrandione and cyclohexanetrione compounds, which are suitable for use as herbicides.Type: GrantFiled: December 12, 2007Date of Patent: March 25, 2014Assignee: Syngenta Crop Protection LLCInventors: Christopher John Mathews, James Nicholas Scutt, Michel Muehlebach