Ring Nitrogen In The Additional Hetero Ring (e.g., Oxazole, Etc.) Patents (Class 514/340)
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Patent number: 8748627Abstract: The present invention relates to compounds of formula (I), which inhibit acetyl-CoA carboxylase (ACC) and are useful for the prevention or treatment of metabolic syndrome, type II diabetes, obesity, atherosclerosis and cardiovascular diseases in humans.Type: GrantFiled: February 15, 2007Date of Patent: June 10, 2014Assignee: AbbVie Inc.Inventors: Yu Gui Gu, Moshe Weitzberg, Xiangdong Xu, Richard F. Clark, Tianyuan Zhang, Qun Li, Todd M. Hansen, Hing Sham, Bruce A. Beutel, Heidi S. Camp, Xiaojun Wang
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Patent number: 8748412Abstract: Provided herein are non-peptide GLP-1 receptor modulator compounds, for example, of Formula I, pharmaceutical compositions comprising such compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of a metabolic disorder.Type: GrantFiled: February 2, 2011Date of Patent: June 10, 2014Assignee: Argusina Bioscience Inc.Inventors: Jiayu Liao, Yufeng Hong, Yong Wang, Thomas W. Von Geldern, Kanyin E. Zhang
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Patent number: 8748340Abstract: This document discloses pesticidal compostions comprising molecules having the following formulas: and processes related thereto.Type: GrantFiled: February 8, 2012Date of Patent: June 10, 2014Assignee: Dow AgroSciecnes LLC.Inventors: Gary D. Crouse, William Thomas Lambert, Thomas C. Sparks, Vidyadhar B. Hegde
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Publication number: 20140155370Abstract: The invention generally relates to the field of nuclear transport modulators, e.g., CRM1 inhibitors, and more particularly to new substituted-heterocyclic azole compounds, the synthesis and use of these compounds and their pharmaceutical compositions, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with CRM1 activity such as in treating cancer and other neoplastic disorders, inflammatory diseases, disorders of abnormal tissue growth and fibrosis including cardiomyopathy, pulmonary fibrosis, hepatic fibrosis, glomerulonephritis, and other renal disorders, and for the treatment of viral infections (both acute and chronic).Type: ApplicationFiled: June 28, 2013Publication date: June 5, 2014Inventors: Sharon Shacham, Michael Kauffman, Vincent P. Sandanayaka, Sharon Shechter
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Publication number: 20140155436Abstract: The present invention relates to a compound of one of the formulas I to XXI; a pharmaceutical composition comprising at least one such compound; and the use of at least one such compound in preparing a drug to treat, in a subject, a genetic disease resulting from at least one splicing anomaly.Type: ApplicationFiled: November 4, 2013Publication date: June 5, 2014Applicants: CENTRE NATIONAL DE RECHERCHE SCIENTIFIQUE, UNIVERSITE MONTPELLIER 2 SCIENCES ET TECHNIQUES, INSTITUT CURIEInventors: Jamal TAZI, David GRIERSON, Florence MAHUTEAU-BETZER, Pierre ROUX
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Patent number: 8742118Abstract: Methods for the synthesis of 2-alkoxy-5-(pyridin-2-yl)pyridine of formula I or salts thereof are provided.Type: GrantFiled: October 18, 2012Date of Patent: June 3, 2014Assignee: F.I.S.—Fabbrica Italiana Sintetici S.p.A.Inventors: Francesco Fontana, Paolo Stabile
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Patent number: 8742119Abstract: Compositions comprising compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are methods of using the compounds that modulate PKM2 in the treatment of cancer.Type: GrantFiled: October 6, 2011Date of Patent: June 3, 2014Assignee: Agios Pharmaceuticals, Inc.Inventors: Francesco G. Salituro, Jeffrey O. Saunders
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Publication number: 20140148340Abstract: Pesticidal compositions and their uses are disclosed.Type: ApplicationFiled: January 31, 2014Publication date: May 29, 2014Applicant: Dow AgroSciences LLCInventors: Annette V. Brown, Gary D. Crouse, Thomas C. Sparks, CaSandra L. McLeod, Emily M. Rigsbee, William T. Lambert, Noormohamed M. Niyaz
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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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Patent number: 8735362Abstract: The present invention relates to compounds of formula (I): Wherein A1, A2, A3, A4, G1, L, Y1, Y2, Y3, Y4, R1, R2, R3 and R4 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to intermediates for preparing compounds of formula (I), to compositions comprising them and to methods of using them to combat and control insect, acarine, nematode and mollusc pests.Type: GrantFiled: December 1, 2010Date of Patent: May 27, 2014Assignee: Syngenta Crop Protection, LLCInventors: Jerome Yves Cassayre, Peter Renold, Myriem El Qacemi, Thomas Pitterna, Julie Clementine Toueg
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Patent number: 8735398Abstract: The present disclosure is generally directed to antiviral compounds, and more specifically directed to compounds which can inhibit the function of the NS5A protein encoded by Hepatitis C virus (HCV), compositions comprising such compounds, and methods for inhibiting the function of the NS5A protein.Type: GrantFiled: November 7, 2012Date of Patent: May 27, 2014Assignee: Bristol-Myers Squibb CompanyInventors: Omar D. Lopez, Denis R. St. Laurent, Jason Goodrich, Jeffrey Lee Romine, Michael Serrano-Wu, Fukang Yang, Ramesh Kakarla, Xuejie Yang, Yuping Qiu, Lawrence B. Snyder
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Patent number: 8735432Abstract: The invention concerns compounds of general formula (I), wherein n, X1, X2, X3, X4, Y and W are as defined herein. The invention also concerns a method for preparing said compounds and their therapeutic use.Type: GrantFiled: October 23, 2012Date of Patent: May 27, 2014Assignee: SanofiInventors: Laurent Dubois, Yannick Evanno, Andre Malanda
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Patent number: 8735399Abstract: The invention provides oxazolidine and thiazolidine derivatives that are useful as subtype selective alpha 2 adrenergic agonists. As such, the compounds described herein are useful in treating a wide variety of disorders associated with selective subtype modulation of alpha 2 adrenergic receptors.Type: GrantFiled: January 14, 2009Date of Patent: May 27, 2014Assignee: Allergan, Inc.Inventors: Todd M. Heidelbaugh, Ken Chow, Santosh C. Sinha, Phong X. Nguyen, Wenkui K. Fang, Ling Li, Janet A. Takeuchi, Smita S. Bhat
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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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Publication number: 20140142105Abstract: The invention relates to novel trifluoromethyl-oxadiazole derivatives of formula (I), and pharmaceutically acceptable salts thereof, (I) in which all of the variables are as defined in the specification, pharmaceutical compositions thereof, pharmaceutical combinations thereof, and their use as medicaments, particularly for the treatment of neurodegeneration, muscle atrophy or metabolic syndrome via inhibition of HDAC4.Type: ApplicationFiled: July 6, 2012Publication date: May 22, 2014Applicant: NOVARTIS AGInventors: Christina Hebach, Emilie Joly, Joerg Kallen, James Gilbert Ternois, Marina Tintelnot-Blomley
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Publication number: 20140142074Abstract: The invention relates to inhibitors of the phosphodiesterase 4 (PDE4) enzyme. More particularly, the invention relates to compounds that are derivatives of 1-phenyl-2-pyridinyl alkyl alcohols, methods of preparing such compounds, compositions containing them and therapeutic use thereof.Type: ApplicationFiled: January 27, 2014Publication date: May 22, 2014Applicant: Chiesi Farmaceutici S.p.A.Inventors: Elisabetta ARMANI, Gabriele Amari, Carmelida Capaldi, Oriana Esposito, Ilaria Peretto
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Publication number: 20140142143Abstract: The invention relates to substituted phenylureas and phenylamides, to processes for the preparation thereof, to pharmaceutical compositions containing these compounds and also to the use of these compounds for preparing pharmaceutical compositions.Type: ApplicationFiled: October 24, 2013Publication date: May 22, 2014Applicant: Gruenenthal GmbHInventors: Robert FRANK, Gregor BAHRENBERG, Thomas CHRISTOPH, Klaus SCHIENE, Jean DE VRY, Nils DAMANN, Sven FRORMANN, Bernhard LESCH, Jeewoo LEE, Yong-Soo KIM, Myeong-Seop KIM, Derek SAUNDERS, Hannelore STOCKHAUSEN
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Patent number: 8729271Abstract: The present invention aims to provide novel compounds of formula [I] or pharmaceutically acceptable salts thereof that are based on a glycine uptake inhibiting action and which are useful in the prevention or treatment of such diseases as schizophrenia, Alzheimer's disease, cognitive dysfunction, dementia, anxiety disorders (generalized anxiety disorder, panic disorder, obsessive-compulsive disorder, social anxiety disorder, posttraumatic stress disorder, specific phobia, acute stress disorder, etc.Type: GrantFiled: September 16, 2011Date of Patent: May 20, 2014Assignee: Taisho Pharmaceutical Co., LtdInventors: Minoru Moriya, Akito Yasuhara, Kazunari Sakagami, Hiroshi Ohta, Kumi Abe, Shuji Yamamoto, Yuko Araki, Hiroki Urabe, Xiang-Min Sun
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Patent number: 8729103Abstract: One aspect of the present invention relates to heterocyclic compounds that are ligands for nicotinic acetylcholine receptors. A second aspect of the invention relates to the use of a compound of the invention for modulation of a mammalian nicotinic acetylcholine receptor.Type: GrantFiled: May 26, 2009Date of Patent: May 20, 2014Assignee: Georgetown UniversityInventors: Milton L. Brown, Mikell A. Paige, Yingxian Xiao, Kenneth J. Kellar
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Patent number: 8729107Abstract: Embodiments of the present disclosure provide a novel pyridine, pharmaceutical compositions comprising such pyridine, and the use of such compositions in treating injured mammalian nerve tissue, including but not limited to an injured spinal cord. In at least one embodiment of the method, the method comprises the step of administering to the mammal in need thereof with a pharmaceutical composition, or pharmaceutically acceptable salt, comprising 4-aminopyridine-3-methanol.Type: GrantFiled: September 9, 2010Date of Patent: May 20, 2014Assignee: Purdue Research FoundationInventors: Richard B. Borgens, Riyi Shi, Stephen R. Byrn, Daniel T. Smith
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Patent number: 8729104Abstract: The instant invention provides compounds of formula I which are 5-lipoxygenase activating protein inhibitors. Compounds of formula I are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.Type: GrantFiled: February 7, 2011Date of Patent: May 20, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Lin Chu, Ihor E. Kopka, Bing Li, Anthony K. Ogawa, Feroze Ujjainwalla
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Patent number: 8729105Abstract: The present invention relates to compounds of the formula wherein A1, A2, A3 and R1 to R8 are defined in the description, and to pharmaceutically acceptable salts thereof, their manufacture, pharmaceutical compositions containing them and their use as medicaments for the treatment and/or prophylaxis of diseases which can be treated with HDL-cholesterol raising agents, such as particularly dyslipidemia, atherosclerosis and cardiovascular diseases.Type: GrantFiled: September 7, 2011Date of Patent: May 20, 2014Assignee: Hoffmann La-Roche Inc.Inventors: Paul Hebeisen, Hugues Matile, Stephan Roever, Matthew Wright, Sannah Zoffmann Jensen
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Publication number: 20140135329Abstract: The present invention provides pyridine and pyrazine derivatives which restore or enhance the function of mutant and/or wild type CFTR to treat cystic fibrosis, primary ciliary dyskinesia, chronic bronchitis, chronic obstructive pulmonary disease, asthma, respiratory tract infections, lung carcinoma, xerostomia and keratoconjunctivitis sire, or constipation (IBS, IBD, opioid induced). Pharmaceutical compositions comprising such derivatives are also encompassed.Type: ApplicationFiled: June 20, 2013Publication date: May 15, 2014Inventors: Urs BAETTIG, Kamlesh BALA, Emma BUDD, Lee EDWARDS, Catherine HOWSHAM, Glyn Alan HUGHES, Darren Mark LEGRAND, Katrin SPIEGEL
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Publication number: 20140134235Abstract: The present invention provides, among other things, new benzylamine compounds, compositions comprising benzylamine compounds, methods of making benzylamine compounds, and methods of using benzylamine compounds for treating or preventing a variety of conditions or diseases associated with lipoprotein metabolism.Type: ApplicationFiled: October 14, 2013Publication date: May 15, 2014Applicant: DR. REDDY'S LABORATORIES LTD.Inventors: Anima BARUAH, Dibyendu DE, Ish Kumar KHANNA, Sivaram PILLARISETTI, Santanu MAITRA, Christopher W. ALEXANDER, Jennepalli SREENU, Indu Dagar, Shanavas Alikunju
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Publication number: 20140135364Abstract: Pesticidal compositions and their uses are disclosed.Type: ApplicationFiled: January 17, 2014Publication date: May 15, 2014Applicant: Dow AgroSciences LLCInventors: William T. Lambert, Gary D. Crouse, Thomas C. Sparks, Denise P. Cudworth
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Publication number: 20140134262Abstract: The present invention provides a compound of Formula I: for use in the treatment, amelioration and/or prevention of diseases and conditions associated with CETP activity, such as atherosclerosis and dyslipidemia, in a subject with high triglyceride level; wherein R1, X1, R7, R5, C, L and p are defined herein. The present invention further provides a combination of pharmacologically active agents for use in the treatment, amelioration and/or prevention of diseases and conditions associated with CETP activity, such as atherosclerosis and dyslipidemia, in a subject with high triglyceride levels.Type: ApplicationFiled: July 6, 2012Publication date: May 15, 2014Inventors: Yoshie Arai, Margaret Elizabeth Brousseau, Jessie Gu, Tomoko Hayashi, Hironobu Mitani, Muneto Mogi, Kazuhiko Nonomura, Ken Yamada
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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: 20140128397Abstract: The present invention provides methods for inhibiting growth and proliferation of HIF pathway proficient cells by administering GLUT1 inhibitors of the invention to HIF pathway proficient cells.Type: ApplicationFiled: January 20, 2012Publication date: May 8, 2014Inventors: John Irwin, Patrick Sutphin, Denise Chan, Sandra Turcotte, Amato Giaccia, Edwin Lai, Olga Razorenova, Michael Patrick Hay, Muriel Bonnet, Connie Sun, Raymond Tabibiazar
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Publication number: 20140128427Abstract: Provided are a novel derivative of 5-carbamoyl adamantan-2-yl amide or a pharmaceutically acceptable salt thereof, and a pharmaceutical use thereof for inhibiting the activity of 11?-hydroxystreroid dehydrogenase type 1 (11b-HSD1) or for preventing and/or treating various diseases mediated by 11?-hydroxystreroid dehydrogenase type 1.Type: ApplicationFiled: June 11, 2012Publication date: May 8, 2014Applicant: SK BIOPHARMACEUTICALS CO., LTD.Inventors: Coo-Min Chung, Choon-Ho Ryu, Yoon-Kyeong Lee, Jin-Sook Moon, Hye-Sung Lee, Seon-Jeong Lee, Kyung-Seok Oh
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Publication number: 20140121194Abstract: There is provided a method for controlling an animal ectoparasite having excellent controlling effects. The method for controlling an ectoparasite of dogs comprises orally administering an ectoparasite-controlling agent comprising as an active ingredient an isoxazoline compound represented by formula (I): wherein X1 represents a halogen atom or a C1-C3 haloalkyl, X2 represents a hydrogen atom, a halogen atom or a C1-C3 haloalkyl, X3 represents a hydrogen atom or a halogen atom, Q represents, for example, Q1, A1 represents R11—C(?O)—N(R12)—N(R13)—, R11—C(?O)—N(R12)—CH2— or R11—C(?O)—N(R12)—, and R10 represents a hydrogen atom, a halogen atom or a C1-C3 alkyl group, to a dog in a period from 30 minutes immediately before the start of feeding to 120 minutes after the end of feeding.Type: ApplicationFiled: October 17, 2013Publication date: May 1, 2014Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Kaori IKARI, Naonobu NISHIGUCHI
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Publication number: 20140120147Abstract: The invention relates to new isoxazoline compounds of formula wherein the variables have the meaning as indicated in the claims; in free form and in salt form; and optionally the enantiomers and geometrical isomers thereof. The compounds of formula (I) are useful in the control of parasites, in particular ectoparasites, in and on warm-blooded animals.Type: ApplicationFiled: January 6, 2014Publication date: May 1, 2014Applicant: NOVARTIS AGInventors: Steve NANCHEN, Noelle GAUVRY, Thomas GOEBEL
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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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Patent number: 8710083Abstract: The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein Y, L, X1, X2, Z, R3, R4, 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: GrantFiled: March 29, 2010Date of Patent: April 29, 2014Assignee: Synta Pharmaceuticals Corp.Inventors: Jun Jiang, Zhi-Qiang Xia, Junyi Zhang, Gary Bohnert, Shoujun Chen, Yu Xie
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Patent number: 8710084Abstract: The present invention provide a tetrazolyl oxime derivative represented by formula (1) (in formula (1), X represents a halogen atom or the like, n1 represents an integer of 0 to 5, A represents a tetrazolyl group, Het represents a group represented by formula (4) or the like, in formula (4), R represents a halogen atom or the like, n2 represents an integer of 0 to 3, Z represents a group represented by formula (a), in formula (a), R50-R53 represents a hydrogen atom or the like, n3 represents an integer of 0 to 2, n4 represents 1 or 2, n5 represents 0 or 1) or salt thereof, and a plant disease control agent containing the same as an active ingredient.Type: GrantFiled: February 26, 2010Date of Patent: April 29, 2014Assignee: Nippon Soda Co., Ltd.Inventors: Syuichi Ito, Kazushige Fujii, Hiroyasu Hosokawa, Ichirou Urihara, Atsunori Isshiki
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Patent number: 8710231Abstract: There is provided a novel oxazolone derivative having inhibitory activity against casein kinase 1? and casein kinase 1?. In addition, the present inhibitor inhibits casein kinase 1? and casein kinase 1?, and thus there is also provided a pharmaceutical agent useful for the treatment and/or prevention of diseases, with the pathological conditions of which the activation mechanism of casein kinase 1? or casein kinase 1? is associated. There is further provided a pharmaceutical agent useful for the treatment of, particularly, circadian rhythm disorder (including sleep disorder), central neurodegenerative disease, and cancer. An inhibitor of casein kinase 1? and casein kinase 1? comprising, as an active ingredient, an oxazolone derivative represented by the following general formula (1), a salt thereof, a solvate thereof, or a hydrate thereof: wherein X represents a halogen atom which is fluorine, chlorine, bromine or iodine.Type: GrantFiled: August 8, 2011Date of Patent: April 29, 2014Assignees: Pharmadesign, Inc., NB Health Laboratory Co., Ltd.Inventors: Masako Okamoto, Kiyoshi Takayama
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Publication number: 20140113931Abstract: Provided are picolinamide compounds for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibiting Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity.Type: ApplicationFiled: March 15, 2013Publication date: April 24, 2014Applicant: Portola Pharmaceuticals, Inc.Inventor: Portola Pharmaceuticals, Inc.
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Publication number: 20140107057Abstract: The present invention provides a combination product comprising a component A and a component B, wherein component A is a compound of formula (I) wherein A1, A2, L, p, R1, R2, R3, R4 and R5 are as defined in claim 1 and component B is a further therapeutic agent; wherein the combination product is for use in a method of therapeutic treatment.Type: ApplicationFiled: May 30, 2012Publication date: April 17, 2014Applicant: Syngenta Participations AGInventors: Jerome Yves Cassayre, Myriem El Qacemi
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Publication number: 20140107161Abstract: The present invention provides compounds of formula (I) wherein R1, R2, R2, R3, R4, G1, n, A1, A2, A3, A4, Y1, Y2, and Y3 are as defined in the claims. The invention also relates to processes and intermediates for preparing these compounds, to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising these compounds and to methods of using these compounds to control insect, acarine, nematode and mollusc pests.Type: ApplicationFiled: May 12, 2012Publication date: April 17, 2014Applicant: SYNGENTA PARTICIPATIONS AGInventors: Jerome Yves Cassayre, Myriem El Qacemi, Torsten Luksch, Peter Renold
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Publication number: 20140107056Abstract: The present invention provides compounds of formula (I): wherein A1, A2, A3 and A4 are independently of one another C—H, C—R5, or nitrogen; B1—B2—B3—B4 is —CH2—C?N—CH2—, —CH2—N—CH2—CH2—, —CH2—C?CH-0- or —CH?C—CH2-0-; G1 is oxygen or sulfur; L is a single bond or C1-C8alkylene; R1 is hydrogen, C1-C8alkyl, C1-C8alkylcarbonyl-, C1-C8alkoxy, C2-C8alkenyl, C2-C8alkynyl, C1-C8alkoxy-C1-C8alkyl, aryl or aryl substituted by one to three R6, or R1 is heterocyclyl or heterocyclyl substituted by one to three R6 or C1-C8alkoxycarbonyl-; R2 is hydrogen, C1-C8haloalkyl or C1-C8alkyl; R3 is C1-C8haloalkyl; R4 is aryl or aryl substituted by one to three R6, or R4 is heterocyclyl or heterocyclyl substituted by one to three R6; Y1 is CR7R8, C?O or C?S; Y2, Y3 and Y4 are independently CR7R8, C=0, C?S, N—R9, O, S, SO or SO2; wherein at least two adjacent ring atoms in the ring formed by Y1, Y2, Y3 and Y4 are heteroatoms; each R7 and R8 is independently hydrogen, halogen, C1-C8alkyl, or C1-C8haloalkyl; and R5, R6, R7, R8 and R9 aType: ApplicationFiled: May 30, 2012Publication date: April 17, 2014Applicant: SYNGENTA PARTICIPATIONS AGInventors: Jerome Yves Cassayre, Peter Renold, Myriem El Qacemi, Thomas Pitterna, Julie Clementine Toueg
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Patent number: 8697715Abstract: Compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of hyperproliferative, pain and inflammatory diseases. Methods of using compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof, 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: GrantFiled: March 1, 2013Date of Patent: April 15, 2014Assignees: Array BioPharma, Inc., Genentech, Inc.Inventors: James F. Blake, Mark Joseph Chicarelli, Rustam Ferdinand Garrey, John Gaudino, Jonas Grina, David A. Moreno, Peter J. Mohr, Li Ren, Jacob Schwarz, Huifen Chen, Kirk Robarge, Aihe Zhou
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Patent number: 8697732Abstract: The invention relates to novel pyridine derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunosuppressive agents.Type: GrantFiled: April 3, 2012Date of Patent: April 15, 2014Assignee: Actelion Pharmaceuticals Ltd.Inventors: Martin Bolli, David Lehmann, Boris Mathys, Claus Mueller, Oliver Nayler, Beat Steiner, Jörg Velker
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Patent number: 8697733Abstract: The present invention relates to novel pyridine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.Type: GrantFiled: June 20, 2013Date of Patent: April 15, 2014Assignee: Allergan, Inc.Inventors: Wenkui K. Fang, Liming Wang, Evelyn G. Corpuz, Ken Chow, Wha-Bin Im
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Patent number: 8697704Abstract: 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: August 11, 2011Date of Patent: April 15, 2014Assignee: Enanta Pharmaceuticals, Inc.Inventors: Yao-Ling Qiu, Xiaowen Peng, Ce Wang, Yat Sun Or
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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: 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: 8691821Abstract: 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, agonists and partial agonists for the mGluR5 receptor and may be useful for the treatment of various disorders of the central nervous system.Type: GrantFiled: November 2, 2011Date of Patent: April 8, 2014Assignee: Bristol-Myers Squibb CompanyInventors: Andrew P. Degnan, Hong Huang, Lawrence B. Snyder, Fukang Yang, Kevin W. Gillman, Michael F. Parker
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Publication number: 20140094462Abstract: Sonic Hedgehog modulators and methods of use thereof are provided for.Type: ApplicationFiled: February 28, 2013Publication date: April 3, 2014Inventors: Sara Buhrlage, Chris Dockendorff, Mike Foley, Han-Je Kim, Andrew Germain, Lawrence MacPherson, Partha Nag, Stuart Schreiber, Amal Ting, Michel Weiwer, Willmen Youngsaye
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Patent number: 8686155Abstract: The present invention relates to chemical compounds having a general formula I wherein A1, A2, C1, C2, D, L1, L2, Z and R3, R4, R6, R7 and R8 are defined herein, which are capable of modulating Aurora kinase protein activity, thereby influencing various disease states and conditions related to the activities of Aurora kinase proteins. For example, the compounds are capable of influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, processes of preparing compounds of the invention, synthetic intermediates and methods of treatment of conditions related to the activity of Aurora kinase.Type: GrantFiled: June 28, 2011Date of Patent: April 1, 2014Assignee: Amgen Inc.Inventors: Victor J. Cee, Philip R. Olivieri, Laurie Schenkel
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Publication number: 20140087943Abstract: The present invention relates to pesticidal mixtures comprising as active compounds 1) at least one isoaxazoline compound I of the formula (I) wherein R1, R2, R3, R4, R5 and A are defined in the description; and 2) at least one active compound II selected from a group A comprising acteylcholine esterase inhibitors, GABA-gated chloride channel antagonists, sodium channel modulators, nicotinic acteylcholine receptor agonists/antagonists, chloride channel activators, juvenile hormone mimics, compounds affecting the oxidative phosphorylation, inhibitors of the chitin biosynthesis, moulting disruptors, inhibitors of the MET, voltage-dependent sodium channel blockers, inhibitors of the lipid synthesis and other compounds as defined in the description, in synergistically effective amounts.Type: ApplicationFiled: September 24, 2013Publication date: March 27, 2014Applicant: BASF SEInventors: Karsten KOERBER, Florian KAISER, Juergen LANGEWALD
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Publication number: 20140088148Abstract: Small molecule inhibitors of XBP1 splicing by IRE1 are provided, as well as methods for their use in treating or preventing cancer (e.g., endocrine resistant breast cancer), diabetes, and obesity.Type: ApplicationFiled: April 4, 2012Publication date: March 27, 2014Applicant: GEORGETOWN UNIVERSITYInventors: Sivanesan Dakshanamurthy, Milton L. Brown, Robert Clarke, Ayesha N. Shahjahan, Jaqueline Smith