1,2-diazines Which Contain An Additional Hetero Ring Patents (Class 544/238)
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Patent number: 9029531Abstract: Compounds and compositions comprising compounds that inhibit glutaminase are described herein. Also described herein are methods of using the compounds that inhibit glutaminase in the treatment of cancer.Type: GrantFiled: November 21, 2013Date of Patent: May 12, 2015Assignee: Agios Pharmaceuticals, Inc.Inventors: Rene M. Lemieux, Janeta Popovici-Muller, Francesco G. Salituro, Jeffrey O. Saunders, Jeremy Travins, Yongsheng Chen
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Publication number: 20150126517Abstract: Novel aryl, heteroaryl, and non-aromatic heterocyle substituted tetrahydroisoquinolines are described in the present invention. These compounds are used in the treatment of various neurological and physiological disorders. Methods of making these compounds are also described in the present invention.Type: ApplicationFiled: January 9, 2015Publication date: May 7, 2015Inventors: Shuang Liu, Bruce F. Molino, Kassoum Nacro
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Publication number: 20150126502Abstract: The present invention provides compounds having a structure according to Formula (I): or a salt or solvate thereof, wherein ring A, X, R1, R2, R3, R4, R5 and R6, are defined herein. The invention further provides pharmaceutical compositions including the compounds of the invention and methods of making and using the compounds and compositions of the invention, e.g., in the treatment and prevention of various disorders, such as Parkinson's disease.Type: ApplicationFiled: January 14, 2015Publication date: May 7, 2015Inventors: Robert A. GALEMMO, Dean R. ARTIS, Xiaocong Michael YE, Danielle Aubele, Anh TRUONG, Simeon BOWERS, Roy K. Hom, Yong-Liang ZHU, R. Jeffrey NEITZ, Jennifer SEALY, Marc ADLER, Paul BEROZA, John P. ANDERSON
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Publication number: 20150126516Abstract: A piperidine compound represented by the following Formula (1): wherein ring A, ring B, and ring C are the same or different and each represent a benzene ring or a nitrogen-containing heteroaromatic ring; W represents a C1-C4 alkylene or alkenylene group; X, Y, and Z are the same or different and each represent a halogen atom, a C1-C6 alkyl group, a halo C1-C6 alkyl group, a C1-C6 alkoxy group, or a halo C1-C6 alkoxy group; m, n, and p are the same or different and each represent an integer of 0 to 5; when m is greater than or equal to 2, the Xs are the same or different; when n is greater than or equal to 2, the Ys are the same or different; and when p is greater than or equal to 2, the Zs are the same or different has an excellent controlling efficacy against pests.Type: ApplicationFiled: April 12, 2013Publication date: May 7, 2015Inventor: Sadayuki Arimori
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Publication number: 20150126506Abstract: 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 PI3 kinase activity, are described herein.Type: ApplicationFiled: January 8, 2015Publication date: May 7, 2015Inventors: 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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Patent number: 9023872Abstract: The present invention relates to substituted triazoles of formula (I), uses thereof, processes for the preparation thereof and compositions containing said compounds. These inhibitors have utility in a variety of therapeutic areas including sexual dysfunction.Type: GrantFiled: May 23, 2012Date of Patent: May 5, 2015Assignee: Ixchelsis LimitedInventors: Alan Daniel Brown, Andrew Antony Calabrese, David Ellis
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Patent number: 9023874Abstract: The invention relates to alkylsulfide derivatives compounds of formula I as hereunder depicted or the enantiomers or veterinarily acceptable salts thereof which are useful for combating or controlling invertebrate pests, in particular arthropod pests and nematodes. The invention also relates to methods for controlling invertebrate pests by using these compounds and to plant propagation material and to agricultural and veterinary compositions comprising said compounds. wherein U, R1, R2, R3U, X, n and p are defined as in the description.Type: GrantFiled: November 11, 2010Date of Patent: May 5, 2015Assignee: Merial, Inc.Inventors: Sebastian Soergel, Ralph Paulini, Steffen Gross, Carsten Beyer, Matthias Pohlman, Henricus Maria Martinus Bastiaans, Michael Rack, Deborah L. Culbertson, Douglas D. Anspaugh, Sarah Thompson, Vincent Salgado
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Publication number: 20150119402Abstract: The present application is related to compounds represented by Formula I, which are novel positive allosteric modulators of al nAChRs. The application also discloses the treatment of disorders that are responsive to enhancement of acetylcholine action on al nAChRs in a mammal by administering an effective amount of a compound of Formula I.Type: ApplicationFiled: May 8, 2013Publication date: April 30, 2015Inventor: Derk Hogenkamp
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Publication number: 20150119387Abstract: The present invention relates to a compound having the structure of Formula I as inhibitor of WNT signal transduction pathways, as well as a composition comprising the compound. Further, the present invention relates to the use of the compound and the method of inhibiting the WNT signal transduction pathways.Type: ApplicationFiled: June 15, 2012Publication date: April 30, 2015Applicant: Curegenix Inc.Inventor: Songzhou An
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Publication number: 20150119384Abstract: The present invention relates to ethynyl derivatives of formula I X, O, R1, R2, R3, R3?, R4, R4?, R5, R6, R6?, m, and n are as defined hereinor to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. Compounds of formula I are positive allosteric modulators (PAM) of the metabotropic glutamate receptor subtype 5 (mGluR5). They can be used for the treatment of schizophrenia or cognitive disorders.Type: ApplicationFiled: January 6, 2015Publication date: April 30, 2015Inventors: Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Heinz Stadler, Eric Vieira
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Patent number: 9018212Abstract: The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD.Type: GrantFiled: May 23, 2011Date of Patent: April 28, 2015Assignee: Boehringer Ingelheim International GmbHInventors: Heiner Ebel, Sara Frattini, Riccardo Giovannini, Christoph Hoenke, Stefan Scheuerer
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Patent number: 9018214Abstract: The invention relates to bicyclic heterocycle compounds of formula (I): or tautomeric or stereochemically isomeric forms, N-oxides, pharmaceutically acceptable salts or the solvates thereof; wherein R1, R2a, R2b, R3a, R3b, R5, R6, R7, R8, R9, p and E are as defined herein; to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.Type: GrantFiled: April 20, 2012Date of Patent: April 28, 2015Assignee: Astex Therapeutics LimitedInventors: Alison Jo-Anne Woolford, Steven Howard, Ildiko Maria Buck, Gianni Chessari, Christopher Norbert Johnson, Emiliano Tamanini, James Edward Harvey Day, Elisabetta Chiarparin, Thomas Daniel Heightman, Martyn Frederickson, Charlotte Mary Griffiths-Jones
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Patent number: 9018224Abstract: Substituted cyclopropyl compounds of the formula (I): and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included.Type: GrantFiled: November 9, 2012Date of Patent: April 28, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Scott Edmondson, Zhiyong Hu, Ping Liu, Gregori J. Morriello, Jason W. Szewczyk, Bowei Wang, Liping Wang, Harold B. Wood, Cheng Zhu, Yuping Zhu, Zhiqiang Guo
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Publication number: 20150111867Abstract: The present invention relates to aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives of the formula (I) or a physiologically tolerated salt thereof The invention relates to pharmaceutical compositions comprising such aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives, and the use of such aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquin oline derivatives for therapeutic purposes. The aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives are GlyT1 inhibitors.Type: ApplicationFiled: October 17, 2014Publication date: April 23, 2015Inventors: Wilhelm Amberg, Frauke Pohlki, Udo Lange, Ying Wang, Jason Brewer, Anil Vasudevan, Yanbin Lao, Charles Hutchins, Hongyu Zhao, Huan-Qiu Li
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Publication number: 20150111750Abstract: N-(tetrazol-5-yl)- and N-(triazol-5-yl)hetarylcarboxamides of formula I and their use as herbicides. The invention relates to N-(tetrazol-5-yl)- and N-(triazol-5-yl)hetarylcarboxamides of formula I and their use as herbicides. In said formula I, B represents N or CH, whereas X1 is N or CR1, X2 is N or CR2, X3 is N or CR3 and X4 is N or CR4; provided that a least one of X1, X3 and X4 is N; R, R1, R2, R3, R4 and R5 represent groups such as hydrogen, halogen or organic groups such as alkyl or phenyl.Type: ApplicationFiled: April 16, 2013Publication date: April 23, 2015Inventors: Helmut Kraus, Matthias Witschel, Thomas Seitz, Trevor William Newton, Liliana Parra Rapado, Klaus Kreuz, Johannes Hutzler, Maciej Pasternak, Jens Lerchl, Richard Roger Evans
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Patent number: 9012445Abstract: 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: GrantFiled: January 12, 2013Date of Patent: April 21, 2015Assignee: Vanderbilt UniversityInventors: Craig W. Lindsley, P. Jeffrey Conn, Michael R. Wood, Bruce J. Melancon, Michael S. Poslusney, James C. Tarr
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Patent number: 9012451Abstract: The present invention relates to 1-aza-bicycloalkyl derivatives of formula I, wherein X is CH2 or a single bond; Y is a group of formula and wherein R has the meanings as defined in the specification, which compounds are alpha 7 nicotinic acetylcholine receptor (nAChR) agonists; to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them.Type: GrantFiled: May 2, 2012Date of Patent: April 21, 2015Assignee: Novartis AGInventors: Dominik Feuerbach, Konstanze Hurth, Timothy John Ritchie
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Publication number: 20150105393Abstract: The present invention relates to amide derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which voltage gated sodium channels are involved.Type: ApplicationFiled: April 25, 2013Publication date: April 16, 2015Inventors: Tatsuya Yamagishi, Kiyoshi Kawamura, Mikio Morita
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Publication number: 20150105548Abstract: The present invention relates to anti-HCV compounds, compositions comprising the same and methods of using the same to treat HCV infection.Type: ApplicationFiled: May 25, 2012Publication date: April 16, 2015Inventors: Allan Krueger, Warren M. Kati, Clarence J. Maring, Rolf Wagner, Charles W. Hutchins
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Publication number: 20150105394Abstract: Compounds of Formula I are provided, including pharmaceutically acceptable salts thereof: wherein A is selected from the group consisting of: wherein Z is selected from the group consisting of: which are useful as HIV attachment inhibitors.Type: ApplicationFiled: March 13, 2013Publication date: April 16, 2015Inventors: Tao Wang, John F. Kadow, Nicholas A. Meanwell, Lawrence G. Hamann
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Publication number: 20150105397Abstract: The present inventions relate to substituted piperazine derivatives of general formula (I) and to the manufacture of said compounds, pharmaceutical compositions comprising a compound according to general formula (I), and the use of said compounds for the treatment of various medical conditions related to glycine transporter-1 (GlyT1).Type: ApplicationFiled: October 14, 2014Publication date: April 16, 2015Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Christoph HOENKE, Riccardo GIOVANNINI, Uta LESSEL, Holger ROSENBROCK, Bernhard SCHMID
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Patent number: 9006228Abstract: Substituted cyclopropyl compounds of the formula I: and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included.Type: GrantFiled: June 11, 2012Date of Patent: April 14, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Michael Miller, Andrew Stamford, Kallol Basu, Harold B. Wood, Duane DeMong, Wanying Sun, Joie Garfunkle, Christopher Moyes, Zhiyong Hu, Ping Liu, Scott D. Edmondson, Xing Dai, Byron Gabriel DuBois
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Patent number: 9006433Abstract: The present invention relates to substituted pyrimidines useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.Type: GrantFiled: April 18, 2011Date of Patent: April 14, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Changyou Zhou, Wuxin Zou, Yuxia Hua, Qun Dang
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Patent number: 9006429Abstract: Pyrandione, thiopyrandione and cyclohexanetrione compounds, which are suitable for use as herbicides.Type: GrantFiled: August 30, 2013Date of Patent: April 14, 2015Assignee: Syngenta Crop Protection, LLCInventors: Christopher John Mathews, James Nicholas Scutt, Michel Muehlebach
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Patent number: 9006269Abstract: Compounds of formula (I) are inhibitors of fatty acid amide hydrolase, (FAAH), and which are useful in the treatment of diseases or medical conditions which benefit from inhibition of FAAH activity, such as anxiety, depression pain, inflammation, and eating, sleep, neurodegenerative and movement disorders: Wherein Ar1 is optionally substituted phenyl or optionally substituted monocyclic heteroaryl having 5 or 6 ring atoms; Ar2 is optionally substituted phenyl, optionally substituted monocyclic heteroaryl having 5 or 6 ring atoms or optionally substituted fused bicyclic heteroaryl having 5 or 6 ring atoms in each fused ring; and Ar3 is a divalent radical selected from the group consisting of optionally substituted phenylene and optionally substituted monocyclic heteroarylene radicals having 5 or 6 ring atoms.Type: GrantFiled: April 19, 2013Date of Patent: April 14, 2015Assignee: Vernalis (R&D) Ltd.Inventors: Stephen Roughley, Steven Walls, Terance Hart, Rachel Parsons, Paul Brough, Christopher Graham, Alba Macias
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Publication number: 20150099756Abstract: The present invention relates to novel compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease, and/or diabetic macular edema.Type: ApplicationFiled: December 15, 2014Publication date: April 9, 2015Inventors: Yun JIN, Zehong WAN, Qing ZHANG
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Publication number: 20150099758Abstract: The present application is related to compounds represented by Formula I, which are novel positive allosteric modulators of al nAChRs. The application also discloses the treatment of disorders that are responsive to enhancement of acetylcholine action on al nAChRs in a mammal by administering an effective amount of a compound of Formula I.Type: ApplicationFiled: May 8, 2013Publication date: April 9, 2015Applicant: Anvyl LLCInventors: David Putnam, Olivier Dasse
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Publication number: 20150099748Abstract: Multiheteroaryl compounds, their preparation, pharmaceutical compositions comprising these compounds, and their pharmaceutical use in the prevention and treatment of prostaglandin D2 mediated diseases and conditions that may be modulated by the inhibition of hematopoietic prostaglandin D synthase (H-PGDS).Type: ApplicationFiled: September 29, 2014Publication date: April 9, 2015Inventors: Gregory W. Endres, Pil Heui Lee, Kirk Lang Olson, James Bernard Kramer, Fred Lawrence Ciske, Stephen Douglas Barrett
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Publication number: 20150094306Abstract: The present invention relates to pyrrolopyridinone derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which voltage gated sodium channels are involved.Type: ApplicationFiled: April 25, 2013Publication date: April 2, 2015Inventors: Kiyoshi Kawamura, Mikio Morita, Tatsuya Yamagishi
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Patent number: 8993567Abstract: Novel cyclic compounds and salts thereof, pharmaceutical compositions containing such compounds, and methods of using such compounds in the treatment of protein tyrosine kinase-associated disorders such as immunologic and oncologic disorders.Type: GrantFiled: March 27, 2014Date of Patent: March 31, 2015Assignee: Bristol-Myers Squibb CompanyInventors: Jagabandhu Das, Ramesh Padmanabha, Ping Chen, Derek Norris, Arthur M. P. Doweyko, Joel C. Barrish, John Wityak
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Publication number: 20150087650Abstract: The present invention relates to 1-aza-bicy-cloalkyl derivatives of Formula (I); wherein the substituents are as defined in the specification, to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them. Formula (I), wherein A represents O or N(R?); Y represents a group of formula, or wherein the left bond is attached to the A group and the right bond is attached to the R group; R represents a substituted or unsubstituted C5-C10aryl, substituted or unsubstituted hetero-C5-C10aryl, a group N(R1)(R4), or a group N(R2)(CHP3R4); R represent a hydrogen, C1-C4alkyl, or CF3; R2 represents hydrogen, C1-C4alkyl, or CF3; R3 represents hydrogen, C1-C4alkyl, or CF3; R4 represents a substituted or unsubstituted C5-C10 aryl or a substituted or unsubstituted C5-C10heteroaryl; in free base or acid addition salt form.Type: ApplicationFiled: December 3, 2014Publication date: March 26, 2015Applicant: NOVARTIS AGInventors: Dominik FEUERBACH, Werner Müller, Bernard Lucien ROY, Thomas TROXLER, Konstanze HURTH, Mathias FREDERIKSEN
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Patent number: 8987453Abstract: The invention relates to compounds that are azaadamantane derivatives, particularly ether- or amine-substituted azaadamantane derivatives and salts and prodrugs thereof, compositions comprising such compounds, methods of using such compounds and compositions, processes for preparing such compounds, and intermediates obtained during such processes.Type: GrantFiled: October 16, 2012Date of Patent: March 24, 2015Assignee: AbbVie Inc.Inventors: Michael R. Schrimpf, Diana L. Nersesian, Kevin B. Sippy, Jianguo Ji, Tao Li, Marc Scanio, Lei Shi, Chih-Hung Lee, William H. Bunnelle, Geoff G. Z. Zhang, Paul J. Brackemeyer, Shuang Chen, Rodger F. Henry
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Patent number: 8987250Abstract: Compounds disclosed herein including compounds of formula I?: and salts thereof are provided. Pharmaceutical compositions comprising compounds disclosed herein, processes for preparing compounds disclosed herein, intermediates useful for preparing compounds disclosed herein and therapeutic methods for treating an HIV infection using compounds disclosed herein are also provided.Type: GrantFiled: April 19, 2013Date of Patent: March 24, 2015Assignee: Gilead Sciences, Inc.Inventors: Kerim Babaoglu, Gediminas Brizgys, Jake Cha, Xiaowu Chen, Hongyan Guo, Randall L. Halcomb, Xiaochun Han, Richard Huang, Hongtao Liu, Ryan McFadden, Michael L. Mitchell, Yingmei Qi, Paul A. Roethle, Lianhong Xu, Hong Yang
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Patent number: 8981085Abstract: Compounds of Formula I are useful for inhibition of CHK1 and/or CHK2. Methods of using compounds of Formula I and stereoisomers and pharmaceutically acceptable salts 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: May 6, 2014Date of Patent: March 17, 2015Assignee: Array BioPharma Inc.Inventors: Yvan Le Huerou, James F. Blake, Indrani W. Gunawardana, Peter J. Mohr, Eli M. Wallace, Bin Wang, Mark Joseph Chicarelli, Michael Lyon
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Patent number: 8980888Abstract: It has been desired to develop a pharmaceutical composition, which is used in agents for preventing and/or treating various diseases related to PDE10 (e.g. mental disorder and neurodegenerative disorder). The present invention provides: compounds having PDE10 inhibitory effect, in particular, compounds having a 4-heteroarylpyrazole-5-carboxylic acid amide structure represented by the following formula (I), or their pharmaceutically acceptable salts, or their solvates; pharmaceutical compositions comprising, as active ingredients, the compounds, or their pharmaceutically acceptable salts, or their solvates; and medical use of the compounds, or their pharmaceutically acceptable salts, or their solvates.Type: GrantFiled: September 4, 2014Date of Patent: March 17, 2015Assignee: Mochida Pharmaceutical Co., Ltd.Inventors: Akihiro Okano, Muneyoshi Makabe, Kouki Ogawa
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Publication number: 20150072860Abstract: The present invention relates to compounds of Formula (I); or an agronomically acceptable salt of said compounds wherein A1a, A1b, A2, A3, A4, X, R1 and R2 are as defined herein. The invention further relates to herbicidal compositions which comprise a compound of Formula (I), and to their use for controlling weeds, in particular in crops of useful plants.Type: ApplicationFiled: March 19, 2013Publication date: March 12, 2015Applicant: SYNGENTA PARTICIPATIONS AGInventor: Glynn Mitchell
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Publication number: 20150072959Abstract: Substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.Type: ApplicationFiled: November 13, 2014Publication date: March 12, 2015Inventors: Dane Goff, Jing Zhang, Catherine Sylvain, Rajinder Singh, Sacha Holland, Jiaxin Yu, Thilo J. Heckrodt, Pingyu Ding
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Publication number: 20150072986Abstract: The present invention provides novel compounds of any one of Formulae (I)-(III), and pharmaceutical compositions thereof. Also provided are particles (e.g., nanoparticles) comprising compounds of Formula (I)-(III) and pharmaceutical compositions thereof that are mucus penetrating. The invention also provides methods and kits for using the inventive compounds, and pharmaceutical compositions thereof, for treating and/or preventing diseases associated with abnormal or pathological angiogenesis and/or aberrant signaling of a growth factor (e.g., vascular endothelial growth factor (VEGF)), such as proliferative diseases (e.g., cancers, benign neoplasms, inflammatory diseases, autoimmune diseases) and ocular diseases (e.g., macular degeneration, glaucoma, diabetic retinopathy, retinoblastoma, edema, uveitis, dry eye, blepharitis, and post-surgical inflammation) in a subject in need thereof.Type: ApplicationFiled: June 11, 2014Publication date: March 12, 2015Inventors: Winston Zapanta Ong, Pawel Wojciech Nowak, John Thomas Feutrill, Jinsoo Kim, Minh Ngoc Nguyen, Elizabeth Enlow
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Patent number: 8975398Abstract: Disclosed are compounds which inhibit the activity of NAMPT, compositions containing the compounds and methods of treating diseases during which NAMPT is expressed.Type: GrantFiled: May 10, 2013Date of Patent: March 10, 2015Assignee: AbbVie Inc.Inventors: Todd M. Hansen, Kenton Longenecker, Howard R. Heyman, Michael L. Curtin, Richard F. Clark, Bryan Sorensen, Zhiqin Ji, Kevin Woller, George Doherty, Robin Frey
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Patent number: 8975254Abstract: The present disclosure relates to compounds of formula (I), and pharmaceutically acceptable salts thereof. The present disclosure also relates to compositions and methods of treating comprising compounds of formula (I), and pharmaceutically acceptable salts thereof.Type: GrantFiled: October 27, 2010Date of Patent: March 10, 2015Assignee: Orion CorporationInventors: Gerd Wohlfahrt, Olli Törmäkangas, Harri Salo, Iisa Höglund, Arja Karjalainen, Pia Knuuttila, Patrik Holm, Sirpa Rasku, Anniina Vesalainen
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Publication number: 20150065517Abstract: The present invention provides organic compounds of the following structure; A-L1-B-C-D-L2-E that are useful for treating or preventing conditions or disorders associated with DGAT1 activity in animals, particularly humans.Type: ApplicationFiled: November 10, 2014Publication date: March 5, 2015Applicant: NOVARTIS AGInventors: Michael H. SERRANO-WU, Young-shin KWAK, Wenming LIU
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Publication number: 20150065516Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12 and A are as described herein, compositions including the compounds and methods of using the compounds.Type: ApplicationFiled: October 29, 2014Publication date: March 5, 2015Inventors: Johannes Aebi, Alfred Binggeli, Cornelia Hertel, Anish Ashok Konkar, Holger Kuehne, Bernd Kuhn, Hans P. Maerki, Halyan Wang
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Publication number: 20150065506Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted tetrazolyl, R2 is optionally substituted phenyl, optionally substituted pyridinyl or optionally substituted thienyl, and R3, R4, R5, R6 R7 and R8 are as defined herein. Also provided are methods of using the compounds for treating diseases associated with the P2X3 and/or a P2X2/3 receptor antagonist and methods of making the compounds.Type: ApplicationFiled: August 13, 2014Publication date: March 5, 2015Applicant: ROCHE PALO ALTO LLCInventors: Li Chen, Michael Patrick Dillon, Lichun Feng, Ronald Charles Hawley, Minmin Yang
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Publication number: 20150065507Abstract: The present invention is directed to novel retinoid-related orphan receptor gamma (ROR?) modulators, processes for their preparation, pharmaceutical compositions containing these modulators, and their use in the treatment of inflammatory, metabolic and autoimmune diseases mediated by ROR?.Type: ApplicationFiled: April 25, 2013Publication date: March 5, 2015Applicant: Glaxo Group LimitedInventors: Veronique Birault, Amanda Jennifer Campbell, Stephen Harrison, Joelle Le, Lena Shukla
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Publication number: 20150065500Abstract: Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.Type: ApplicationFiled: September 11, 2014Publication date: March 5, 2015Applicant: Vertex Pharmaceuticals IncorporatedInventors: Sara Hadida-Ruah, Matthew Hamilton, Mark Miller, Peter D.J. Grootenhuis, Brian Bear, Jason McCartney, Jinglan Zhou, Frederick van Goor
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Patent number: 8969553Abstract: Process for the selective N-sulfonylation of oxindoles, in particular process for the N-sulfonylation of 3-triazinyloxindoles, and also N-sulfonyl-substituted 3-triazinyloxindoles and the use of N-sulfonyl-substituted oxindoles and of N-sulfonyl-substituted 3-triazinyloxindoles as intermediates for the synthesis of fine chemicals and of active ingredients in the field of pharmacy and agriculture, and also the use of these compounds as active ingredients in the field of agriculture.Type: GrantFiled: December 19, 2011Date of Patent: March 3, 2015Assignee: Bayer Intellectual Property GmbHInventors: Gunter Karig, Mark James Ford, Konrad Siegel, Stefan Schnatterer
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Publication number: 20150057286Abstract: This invention relates to bis-amido pyridines of general formula (I) their use as SMAC mimetics, pharmaceutical compositions containing them, and their use as a medicaments for the treatment and/or prevention of diseases characterized by excessive or abnormal cell proliferation and associated conditions such as cancer. The groups R1 to R4 have the meanings given in the claims and in the specification.Type: ApplicationFiled: August 20, 2014Publication date: February 26, 2015Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventor: Ulrich REISER
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Publication number: 20150057288Abstract: A pest control method for honeybee parasitic pests has been found, which is highly safe to honeybees and demonstrates excellent pest control effects against honeybee parasitic pests by using a honeybee parasitic pest control agent containing at least one of a compound represented by Formula (I) and acid addition salts thereof.Type: ApplicationFiled: November 10, 2014Publication date: February 26, 2015Applicant: MEIJI SEIKA PHARMA CO., LTD.Inventors: Ryo HORIKOSHI, Masaaki MITOMI
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Patent number: 8962580Abstract: The invention features compounds of formula I or II: In one embodiment, the invention relates compounds and processes for conjugating ligand to oligonucleotide. The invention further relates to methods for treating various disorders and diseases such as viral infections, bacterial infections, parasitic infections, cancers, allergies, autoimmune diseases, immunodeficiencies and immunosuppression.Type: GrantFiled: September 23, 2009Date of Patent: February 24, 2015Assignee: Alnylam Pharmaceuticals, Inc.Inventors: Muthiah Manoharan, Kallanthottathil G. Rajeev, Takeshi Yamada, David Butler, Narayanannair K. Jayaprakash, Muthusamy Jayaraman, Shigeo Matsuda, Rajendra K. Pandey, Chang Geng Peng
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Patent number: 8962625Abstract: A pyridazinone compound represented by the formula (I) has excellent effect on weed control and is useful as an active ingredient of herbicides.Type: GrantFiled: March 22, 2012Date of Patent: February 24, 2015Assignee: Sumitomo Chemical Company, LimitedInventors: Toshiyuki Kiji, Takafumi Fusaka