Pyridine Ring Or Partially Hydrogenated Pyridine Ring Patents (Class 546/193)
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Patent number: 11707456Abstract: The present disclosure relates to a process for preparing arimoclomol, arimoclomol citrate and key intermediates, such as ORZY-01, thereof. The disclosure further relates to a process for preparing high purity arimoclomol citrate and methods of using the same.Type: GrantFiled: March 10, 2022Date of Patent: July 25, 2023Inventors: Zhe Zhang, Mark Read, Elisabeth Vang Carstensen, Marco Poppe, Andreas Pelz
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Patent number: 11369624Abstract: This invention provides for prodrug Compounds I, pharmaceutical compositions thereof, and their use in treating HIV infection. wherein: X is C or N with the proviso that when X is N, R1 does not exist; W is C or N with the proviso that when W is N, R2 does not exist; V is C; E is hydrogen or a pharmaceutically acceptable salt thereof; and Y is selected from the group consisting of Also, this invention provides for intermediate Compounds II useful in making prodrug Compounds I. wherein: L and M are independently selected from the group consisting of C1-C6 alkyl, phenyl, benzyl, trialkylsilyl, -2,2,2-trichloroethoxy and 2-trimethylsilylethoxy.Type: GrantFiled: October 13, 2020Date of Patent: June 28, 2022Inventors: Yasutsugu Ueda, Timothy P. Connolly, John F. Kadow, Nicholas A. Meanwell, Tao Wang, Chung-Pin H. Chen, Kap-Sun Yeung, Zhongxing Zhang, David Kenneth Leahy, Shawn K. Pack, Nachimuthu Soundararajan, Pierre Sirard, Kathia Levesque, Dominique Thoraval
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Patent number: 11332459Abstract: The present invention relates to inhibitors of Transient Receptor Potential Channel 6 (TRPC6) protein activity. The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising a compound of the invention, a method for manufacturing compounds of the invention and therapeutic uses thereof.Type: GrantFiled: October 18, 2018Date of Patent: May 17, 2022Assignee: TEIJIN PHARMA LIMITEDInventors: Michael D. Bartberger, Nagasree Chakka, Hua Gao, Angel Guzman-Perez, Daniel B. Horne, Zihao Hua, Madeleine Kieffer, Daniel C. H. Lin, Benjamin Charles Milgram, Jane Panteleev, Laurie Schenkel, John Stellwagen, Matthew Weiss, Ryan D. White, Wei Zhao
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Patent number: 11179329Abstract: The present invention concerns new therapeutical uses, including low dosage administration of the highly potent H3-ligand: (3S)-4-{4-[3-(3-methylpiperidin-1-yl)propoxy]phenyl}pyridine 1-oxide.Type: GrantFiled: March 21, 2018Date of Patent: November 23, 2021Assignee: BIOPROJET PHARMAInventors: Jeanne-Marie Lecomte, Jean-Charles Schwartz, Olivier Labeeuw, Marc Capet
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Patent number: 11072587Abstract: Novel compositions and methods for the treatment and prevention of malaria are disclosed herein.Type: GrantFiled: September 10, 2018Date of Patent: July 27, 2021Assignee: University of Central Florida Research Foundation, Inc.Inventors: Debopam Chakrabarti, Ratna Chakrabarti
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Patent number: 10961238Abstract: There are described compounds of formula (I): and there use as a medicament in the treatment of conditions involving abnormal activation and/or malfunction of the of the hedgehog pathway, such as cancer, fibrosis and chronic graft-versus-host disease (cGVHD).Type: GrantFiled: October 25, 2017Date of Patent: March 30, 2021Assignee: E-THERAPEUTICS PLCInventors: Maja Ro{hacek over (s)}cic, Filip Kolund{hacek over (z)}ic, Dinko {hacek over (Z)}iher, Tanja Poljak, Srinivasamurthy Vadlamudi, Colin Stubberfield
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Patent number: 10894783Abstract: This disclosure relates to the field of molecules having pesticidal utility against pests in Phyla Arthropoda, Mollusca, and Nematoda, processes to produce such molecules, pesticidal compositions containing such molecules, and processes of using such pesticidal compositions against such pests. These pesticidal compositions may be used, for example, as acaricides, insecticides, miticides, molluscicides, and nematicides. This document discloses a molecule having the following formula.Type: GrantFiled: May 20, 2019Date of Patent: January 19, 2021Assignee: DOW AGROSCIENCES LLCInventors: Yu Zhang, Tony K. Trullinger, Carla J. R. Klittich, Ricky Hunter
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Patent number: 10744125Abstract: Modulators of the adenosine A3 receptors of formula (I): and process for preparing said compounds. Other aspects of the present invention are pharmaceutical compositions comprising an effective amount of said compounds and the use of said compounds in the preparation of a medicament for treating pathological conditions or diseases that can be improved by modulation of adenosine A3 receptors.Type: GrantFiled: January 19, 2018Date of Patent: August 18, 2020Assignee: Palobiofarma, S.L.Inventors: Julio Castro Palomino Laria, Juan Camacho Gómez, Abdelaziz El Maatougui
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Patent number: 10723725Abstract: Provided herein are aminopyridine derivatives and pharmaceutical compositions that are useful as TAM family kinase inhibitors.Type: GrantFiled: January 22, 2019Date of Patent: July 28, 2020Assignee: SignalChem Lifesciences CorporationInventor: Zaihui Zhang
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Patent number: 10597376Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds as exemplified as follows, The subject compounds and compositions are useful for inhibition of lysine specific demethylase-1. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.Type: GrantFiled: May 29, 2018Date of Patent: March 24, 2020Assignee: Celgene Quanticel Research, Inc.Inventors: Young K. Chen, Toufike Kanouni, Jeffrey Alan Stafford, James Marvin Veal
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Patent number: 10442794Abstract: Processes for preparing pyridinecarboxamide derivatives are provided. In particular, process for preparing pyridinecarboxamide derivatives represented by general formula (I) are provided, wherein the substituents of the formula (I) are defined in the specification.Type: GrantFiled: January 25, 2019Date of Patent: October 15, 2019Assignees: Jiangsu Hengrui Medicine Co., Ltd., Shanghai Hengrui Pharmaceutical Co., Ltd.Inventors: Xin Li, Qing Dong, Piaoyang Sun
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Patent number: 10428012Abstract: The present invention relates to a preparation method of 4-isopropylamino-1-butanol, in which using cheap and readily available tetrahydrofuran and acetic acid solution of hydrogen bromide as starting materials to prepare a novel intermediate of 4-isopropylamino-1-acetoxyl butane and further obtain the target product. The present invention has advantages of convenient process operations, mild reaction conditions, economical and environment-friendly benefits, and suitability for industrial production to obtain the product with high purity and high yield.Type: GrantFiled: September 28, 2018Date of Patent: October 1, 2019Assignee: SEASONS BIOTECHNOLOGY CO., LTD.Inventors: Fanghui Tang, Chi Ma, Qiang Jia
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Patent number: 10233176Abstract: Provided herein are aminopyridine derivatives and pharmaceutical compositions that are useful as TAM family kinase inhibitors.Type: GrantFiled: November 26, 2014Date of Patent: March 19, 2019Assignee: SIGNALCHEM LIFESCIENCES CORPORATIONInventor: Zaihui Zhang
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Patent number: 10189788Abstract: The present application relates to novel substituted N,2-diarylquinoline-4-carboxamide derivatives, to processes for preparation thereof, to the use thereof alone or in combinations for treatment and/or prevention of diseases, and to the use thereof for production of medicaments for treatment and/or prevention of diseases, especially for treatment and/or prevention of fibrotic and/or inflammatory disorders.Type: GrantFiled: September 7, 2015Date of Patent: January 29, 2019Assignee: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Hartmut Beck, Tobias Thaler, Raimund Kast, Daniel Meibom, Mark Meininghaus, Carsten Terjung, Martina Delbeck, Klemens Lustig, Uwe Muenster, Britta Olenik
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Patent number: 10150752Abstract: 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: June 28, 2016Date of Patent: December 11, 2018Assignee: Ixchelsis LimitedInventors: Alan Daniel Brown, Andrew Antony Calabrese, David Ellis
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Patent number: 9414594Abstract: The present application provides processes for making pesticidal compounds and compounds useful both as pesticides and in the making of pesticidal compounds.Type: GrantFiled: May 19, 2015Date of Patent: August 16, 2016Assignee: Dow AgroSciences LLCInventors: Qiang Yang, Beth Lorsbach, Gregory Whiteker, Gary Roth, Carl DeAmicis, Daniel I. Knueppel, Ann M. Buysse, Kaitlyn Gray, Xiaoyong Li, Joseck M. Muhuhi, Ronald Ross, Jr., David E. Podhorez, Yu Zhang
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Patent number: 9260663Abstract: A liquid crystal composition is described, including a liquid crystalline compound (A), and at least one nitrogen-containing compound (B) selected from compounds represented by formula (1) and compounds represented by formula (2), wherein R? is a hydrogen atom or a monovalent organic group that is bonded to the nitrogen atom via a chain-shaped hydrocarbon group or an alicyclic hydrocarbon group, R2 and R3 are independently a divalent organic group that is bonded to the nitrogen atom via a chain-shaped hydrocarbon group, an alicyclic hydrocarbon group or *—CO—R4—, A1 is a nitrogen-containing heteroaromatic ring, X1 is a cyclic ether group or a polymerizable unsaturated group, and R10 is a divalent organic group that is bonded to the primary amino group via a chain-shaped hydrocarbon group or an alicyclic hydrocarbon group.Type: GrantFiled: August 7, 2014Date of Patent: February 16, 2016Assignee: JSR CORPORATIONInventors: Hiroaki Tokuhisa, Yuusuke Uesaka
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Patent number: 9242976Abstract: Compounds having the following formula (I) or an enantiomer, diastereomer or a pharmaceutically-acceptable salt thereof, wherein X is N or C—R7, are useful as kinase modulators, including IRAK-4 modulation.Type: GrantFiled: January 11, 2013Date of Patent: January 26, 2016Assignee: Bristol-Myers Squibb CompanyInventors: Venkatram Reddy Paidi, Sreekantha Ratna Kumar, Abhisek Banerjee, Ramesh Sistla, Satheesh Kesavan Nair, William J. Pitts, John Hynes
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Patent number: 9034874Abstract: The invention relates to compound of the formula I or a salt thereof, wherein the substituents are as defined in the specification; to its preparation, to its use as medicament and to medicaments comprising it.Type: GrantFiled: July 17, 2013Date of Patent: May 19, 2015Assignee: NOVARTIS AGInventors: Yves Auberson, Mark Gary Bock, Dario Braga, Marco Curzi, Stephanie Kay Dodd, Stefano Luca Giaffreda, Haiyang Jiang, Piotr Karpinski, Thomas J. Troxler, Tielin Wang, Xiaoyang Wang, Xuechun Zhang
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Publication number: 20150111734Abstract: A pesticidal composition comprises at least one compounds selected from a compound of formula, or any agriculturally acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, Q, Z, L, La, and x are as described herein. A method of controlling pests comprises applying the pesticidal composition near a population of pests.Type: ApplicationFiled: October 17, 2014Publication date: April 23, 2015Inventors: Yu Zhang, Asako Kubota, Noormohamed M. Niyaz, Thomas Barton, Tony K. Trullinger, Christian T. Lowe, Paul R. LePlae, Ann M. Buysse, Martin J. Walsh, Negar Garizi, Ricky Hunter, Daniel Knueppel
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Publication number: 20150111922Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof: (I) in which m, n, W, X, Y, Z, R1, R2, R3 and R4 are as defined in the specification, for use in the treatment or prevention of a diseases o conition mediated by a prokineticin, such as psychiatric and neurological conditions.Type: ApplicationFiled: May 29, 2013Publication date: April 23, 2015Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Colm Carroll, Anne Goldby, Martin Teall
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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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Patent number: 9006446Abstract: This document discloses molecules having the following formula (“Formula I”):Type: GrantFiled: November 14, 2012Date of Patent: April 14, 2015Assignee: Dow AgroSciences LLCInventors: Tony K. Trullinger, Ricky Hunter, Negar Garizi, Maurice C. H. Yap, Ann M. Buysse, Dan Pernich, Timothy C. Johnson, Kristy Bryan, Carl Deamicis, Yu Zhang, Noormohamed M. Niyaz, CaSandra Lee McLeod, Ronald Ross, Jr., Yuanming Zhu, Peter Lee Johnson, Joseph D. Eckelbarger, Marshall H. Parker
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Patent number: 9006266Abstract: Heteroarylpiperidine and -piperazine derivatives of the formula (I) in which the symbols A, X, Y, L1, L2, G, Q, p, R1, R2 and R10 are each as defined in the description, and salts, metal complexes and N-oxides of the compounds of the formula (I), and the use thereof for controlling phytopathogenic harmful fungi and processes for preparing compounds of the formula (I).Type: GrantFiled: August 24, 2011Date of Patent: April 14, 2015Assignee: Bayer Intellectual Property GmbHInventors: Tomoki Tsuchiya, Pierre Wasnaire, Sebastian Hoffmann, Pierre Cristau, Thomas Seitz, Joachim Kluth, Stefan Hillebrand, Juergen Benting, Daniela Portz, Ulrike Wachendorff-Neumann
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Publication number: 20150099743Abstract: The present invention relates to compounds and pharmaceutically acceptable salts of Formulas A and B: wherein A, B, R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are as defined above. The invention further relates to pharmaceutical compositions comprising the compounds and pharmaceutically acceptable salts and to methods of treating diabetes mellitus and its complications, cancer, ischemia, inflammation, central nervous system disorders, cardiovascular disease, Alzheimer's disease and dermatological disease pression, virus diseases, inflammatory disorders, or diseases in which the liver is a target organ.Type: ApplicationFiled: October 3, 2014Publication date: April 9, 2015Inventors: Hui LI, Seiji NUKUI, Stephanie Anne SCALES, Min TENG, Chunfeng YIN
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Patent number: 8993592Abstract: Provided is a cyclic amine compound, represented by the following formula (I) that has superior acaricidal activity, has superior properties and safety, and which can be synthesized industrially advantageously, a salt thereof and an acaricide: (wherein, Cy1 and Cy2 respectively and independently represent, for example, an aryl group, R1a, R1b, R2a, R2b, R3a, R3b, R4a, R4b and R5a respectively and independently represent, for example, a hydrogen atom, R1a and R2a or R3a and R4a may together form, for example, an ethylene group, R10, R11, R20 and R21 respectively and independently represent, for example, an alkyl group, R10 or R11 may respectively or mutually, or together with an atom that bonds on Cy1, form a ring, R20 or R21 on Cy2 may respectively or mutually, or with an atom that bonds on Cy2, form a ring, m represents an integer of 0 to 5, n represents an integer of 0 to 5, p represents an integer of 0 to 5, and r represents an integer of 0 to 5).Type: GrantFiled: December 17, 2010Date of Patent: March 31, 2015Assignee: Nippon Soda Co., Ltd.Inventors: Isami Hamamoto, Keiji Koizumi, Makio Yano, Masahiro Kawaguchi, Hazumi Nomura, Tetsuya Haruyama
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Patent number: 8987457Abstract: The present invention provides a compound of formula (A): as described herein, and pharmaceutically acceptable salts, enantiomers, rotamers, tautomers, or racemates thereof. Also provided are methods of treating a disease or condition mediated by PIM kinase using the compounds of Formula I, and pharmaceutical compositions comprising such compounds.Type: GrantFiled: May 20, 2013Date of Patent: March 24, 2015Assignee: Novartis AGInventors: Matthew Burger, Joseph E. Drumm, III, Gisele Nishiguchi, Alice Rico, Robert Lowell Simmons, Benjamin Taft, Huw Tanner
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Publication number: 20150080367Abstract: The present invention provides for compounds of Formula I and various embodiments thereof, and compositions comprising compounds of Formula I and various embodiments thereof. In compounds of Formula I, the groups R1, R2, R3, R4, R5, R6, m, n and the C-linked Ring have the meaning as described herein. The present invention also provides for methods of using compounds of Formula I and compositions comprising compounds of Formula I as DLK inhibitors and for treating neurodegeneration diseases and disorders.Type: ApplicationFiled: November 21, 2014Publication date: March 19, 2015Applicant: Genentech, Inc.Inventors: Frederick Cohen, Malcolm Huestis, Cuong Ly, Snahel Patel, Michael Siu, Xianrui Zhao
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Patent number: 8980912Abstract: The present invention provides a cyclic amine compound represented by formula (I) (in formula (I), Cy1 and Cy2 independently represent a C6-10 aryl group or a heterocyclyl group; R1a to R5a independently represent a hydrogen atom or an unsubstituted or substituted C1-6 alkyl group; R10, R11, R20 and R21 independently represent an unsubstituted or substituted C1-6 alkyl group, an unsubstituted or substituted C1-6 alkoxy group, a halogen atom or the like; m, n, p, and r each represent an integer of 0 to 5; and Y represents an oxygen atom or the like) or salt thereof, and an acaricide including the same.Type: GrantFiled: February 24, 2011Date of Patent: March 17, 2015Assignee: Nippon Soda Co., Ltd.Inventors: Isami Hamamoto, Keiji Koizumi, Masahiro Kawaguchi, Hisashi Tanigawa, Takehiko Nakamura, Tomomi Kobayashi
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Patent number: 8975286Abstract: The present invention is directed to ether benzotriazole derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.Type: GrantFiled: August 16, 2010Date of Patent: March 10, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Vadim Y. Dudkin, Mark E. Fraley, Cheng Wang, Robert M. Garbaccio, Douglas C. Beshore, Scott K. Kuduk, Jason W. Skudlarek
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Publication number: 20150065715Abstract: The present invention relates to novel amidopyridine derivatives. More specifically, the present invention provides a medicinal agent which is useful as a prophylactic or therapeutic agent for diseases based on the production of cytokines from T cells, comprising as the active ingredient an amidopyridine derivative or a pharmacologically acceptable salt thereof. Provided are an amidopyridine derivative of the following general formula (I): wherein each symbol has the same meaning as defined in the description, or a pharmacologically acceptable salt thereof.Type: ApplicationFiled: April 12, 2013Publication date: March 5, 2015Applicant: Mitsubishi Tanabe Pharma CorporationInventors: Masayuki Watanabe, Hiroyuki Furukawa, Maiko Hamada, Naoto Fujie, Hiroyuki Ushio, Tooru Takashima
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Patent number: 8969383Abstract: The present invention relates to picolinamide 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: GrantFiled: June 12, 2014Date of Patent: March 3, 2015Assignee: RaQualia Pharma Inc.Inventors: Hirohide Noguchi, Tadashi Inoue, Mikio Morita, Yoshimasa Arano
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Publication number: 20150057248Abstract: Embodiments of the invention are directed to compounds that are positive allosteric modulators of AMPA receptors.Type: ApplicationFiled: September 1, 2014Publication date: February 26, 2015Applicant: The Board of Regents of The University of Texas SystemInventors: Jia Zhou, Haijun Chen, Kenneth M. Johnson, Cheng Z. Wang
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Publication number: 20150051226Abstract: The invention, in a first aspect relates to compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein R is a 6-membered aromatic ring, or a 5- or 6-membered heteroaromatic ring comprising 1 to 3 heteroatoms selected from S, O and N, or a 6-membered benzocondensed heteroaromatic ring containing N as heteroatom, optionally each of said rings being substituted with one or two substituents selected from the group consisting of (C1-C3)alkyl, (C3-C5)cycloalkyloxy, (C1-C3)alkylcarbonyl, cyano, trifluoromethyl, dimethylamino, or phenyl which optionally is substituted with one or more halogen atoms, or a 5- or 6-membered heterocycle containing from one to three nitrogen atoms; X is O or N; P is pyridyl, pyrimidyl, pyrazyl, or pyridazyl, each being optionally substituted with one or more substituents selected from the group consisting of (C1-C3)alkyl, halogen, trifluoromethyl, and cyano, and use thereof as pharmaceuticals.Type: ApplicationFiled: February 28, 2013Publication date: February 19, 2015Inventors: Luigi Piero Stasi, Lucio Rovati, Roberto Artusi, Clara Bovino, Fabrizio Colace, Stefano Mandelli
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Patent number: 8957063Abstract: Compounds which modulate the CB2 receptor are disclosed. The compounds are useful for treating CB2 receptor-mediated diseases such as pain.Type: GrantFiled: February 19, 2009Date of Patent: February 17, 2015Assignee: Boehringer Ingelheim International GmbHInventors: Pier Francesco Cirillo, Eugene Richard Hickey, Doris Riether, Monika Ermann, Innocent Mushi
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Publication number: 20150045218Abstract: This document discloses molecules having the following formula (“Formula I”):Type: ApplicationFiled: October 23, 2014Publication date: February 12, 2015Applicant: DOW AGROSCIENCES LLCInventors: Tony K. Trullinger, Ricky Hunter, Negar Garizi, Maurice C. Yap, Ann M. Buysse, Dan Pernich, Timothy C. Johnson, Kristy Bryan, Carl DeAmicis, Yu Zhang, Noormohamed M. Niyaz, CaSandra L. McLeod, Ronald Ross, JR., Yuanming Zhu, Peter Lee Johnson, Joseph D. Eckelbarger, Marshall H. Parker
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Publication number: 20150045347Abstract: Compounds having the following formula: (I) wherein: A is an optionally substituted triazole, or a stereoisomer or a pharmaceutically-acceptable salt thereof, are useful as kinase modulators, including IRAK-4 modulation.Type: ApplicationFiled: January 11, 2013Publication date: February 12, 2015Inventors: Dharmpal S. Dodd, Christopher P. Mussari, Rajeev S. Bhide, Satheesh Kesavan Nair, Venkatram Reddy Paidi, Sreekantha Ratna Kumar, Abhisek Banerjee, Ramesh Sistla, William J. Pitts, John Hynes
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Publication number: 20150031541Abstract: Compounds of the formula (I) wherein the substituents are as defined in claim 1, are useful as a pesticides.Type: ApplicationFiled: February 27, 2013Publication date: January 29, 2015Applicant: Syngenta Participations AGInventors: Clemens Lamberth, Sarah Sulzer-Mosse, Fredrik Cedarbaum, Jayant Umarye, Ravindra Sonawane
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Publication number: 20150028271Abstract: The present invention relates to a compound represented by Formula 1, wherein in Formula 1, each of R1 to R7 is the same as defined in the specification, a photosensitive resin composition comprising the same, and a color filter prepared using the same. The color filter can realize high contrast and high brightness.Type: ApplicationFiled: June 18, 2014Publication date: January 29, 2015Inventors: Myoung Youp SHIN, Won Jung KIM, Hwan Sung CHEON, Eui Soo JEONG
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Publication number: 20150018344Abstract: Compounds having the following formula (I) or an enantiomer, diastereomer or a pharmaceutically-acceptable salt thereof, wherein X is N or C—R7, are useful as kinase modulators, including IRAK-4 modulation.Type: ApplicationFiled: January 11, 2013Publication date: January 15, 2015Inventors: Venkatram Reddy Paidi, Sreekantha Ratna Kumar, Abhisek Banerjee, Ramesh Sistla, Satheesh Kesavan Nair, William J. Pitts, John Hynes
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Publication number: 20150011526Abstract: The present invention relates to 2-oxo-piperidinyl derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.Type: ApplicationFiled: October 10, 2012Publication date: January 8, 2015Inventors: Ali Ates, Florian Montel, Anne Valade, Olivier Lorthioir
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Publication number: 20140371195Abstract: The present application discloses compounds capable of modulating the activity of histone demethylases (HDMEs), which are useful for prevention and/or treatment of diseases in which genomic dysregulation is involved in the pathogenesis, such as e.g. cancer. The present application also discloses pharmaceutical compositions comprising said compounds and the use of such compounds as a medicament.Type: ApplicationFiled: August 28, 2014Publication date: December 18, 2014Inventors: Marc Labelle, Thomas Boesen, Mukund Mehrotra, Qasim Khan, Farman Ullah
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Patent number: 8912218Abstract: The invention relates to the novel products of formula (I): in which: Ra represents H, Hal, aryl or heteroaryl, which is optionally substituted; Rb represents H, Rc, —COORc-CO—Rc or —CO—NRcRd; where Rc represents alkyl, cycloalkyl, heterocycloalkyl, aryl and heteroaryl, all optionally substituted; Rd represents H, alk or cycloalkyl; these products being in all the isomer forms and the salts, as medicaments, in particular as MET inhibitors.Type: GrantFiled: July 21, 2009Date of Patent: December 16, 2014Assignee: SanofiInventors: Ahmed Abouabdellah, Jochen Görlitzer, Peter Hamley, Antoine Ravet
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Publication number: 20140350015Abstract: The present invention relates to pyridine and pyrimidine based compounds, pharmaceutical compositions comprising these compounds and their potential use as therapeutic agents for the treatment and/or prevention of cancer.Type: ApplicationFiled: June 12, 2014Publication date: November 27, 2014Inventors: Edward McDonald, Julian Blagg, Mark Pichowicz, Simon Ross Crumpler
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Patent number: 8889670Abstract: Compounds which modulate the CB2 receptor are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.Type: GrantFiled: February 16, 2010Date of Patent: November 18, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Alessandra Bartolozzi, Angela Berry, Pier Francesco Cirillo, Eugene Richard Hickey, Doris Riether, Lifen Wu, Renee M. Zindell
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Patent number: 8889714Abstract: The present invention relates to 3,4-substituted piperidinyl-based renin inhibitor compounds bearing at 4-position oxopyridine and having the formula (I). The invention further relates to pharmaceutical compositions containing said compounds, as well as their use in treating cardiovascular events and renal insufficiency.Type: GrantFiled: May 4, 2009Date of Patent: November 18, 2014Assignee: Actelion Pharmaceuticals Ltd.Inventors: Austin Chih-Yu Chen, Daniel Dube, Pierre-Andre Fournier, Erich L. Grimm, Patrick Lacombe, Sebastien Laliberte, Dwight Macdonald, D. Bruce MacKay, Daniel James McKay, Tom Yao-Hsiang Wu, Louis-Charles Campeau, Jeremy Peter Scott, Nadine Bremeyer
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Patent number: 8889715Abstract: The present invention provides salt adducts comprising at least one positively charged moiety being a pyridoxine or a derivative thereof and at least one carboxylated 5- to 7-membered lactam ring, optionally additionally substituted, methods of their preparation, and pharmaceutical compositions and medicaments comprising them. Salt adducts of the invention and compositions comprising them may be used to in the treatment of diseases or disorders associated with or inflicted by alcohol consumption.Type: GrantFiled: November 2, 2012Date of Patent: November 18, 2014Assignee: Alcobra Ltd.Inventors: Rina Yamin, Dalia Megiddo
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Publication number: 20140328805Abstract: The present invention provides for compounds of Formula I and embodiments and salts thereof for the treatment of diseases (e.g., neurodegenerative diseases). R1, R2, R3, X1, X2, A and Cy variable in Formula all have the meaning as defined herein.Type: ApplicationFiled: May 1, 2014Publication date: November 6, 2014Applicant: GENENTECH, INC.Inventors: Anthony Estrada, Alan G. Olivero, Snahel Patel, Michael Siu
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Patent number: 8871796Abstract: The invention encompasses a novel class of diaryl ether derivatives which inhibit the processing of APP by the putative ?-secretase while sparing Notch signaling pathway, and thus are useful in the treatment or prevention of Alzheimer's disease without the development of Notch inhibition mediated gastrointestinal issues. Pharmaceutical compositions and methods of use are also included.Type: GrantFiled: October 5, 2010Date of Patent: October 28, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: William Colby Brown, Jason Brubaker, Christian Fischer, Richard W. Heidebrecht, John T. Hendrix, Elizabeth H. Kelley, Rachel N. MacCoss, Joey L. Methot, Thomas Miller, Karin M. Otte, Phieng Siliphaivanh, Thomas Reger, Peter D. Williams, Catherine M. Wiscount
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Patent number: 8859588Abstract: The present disclosure relates to a series of substituted N-heteroaryl bipyrrolidine carboxamides of formula (I). wherein R1, R2, R3, R4, Q1, Q2, Q3, Q4, X, m and p are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this disclosure also relates to methods of preparation of substituted N-heteroaryl bipyrrolidine carboxamides of formula (I) and intermediates therefor.Type: GrantFiled: November 6, 2012Date of Patent: October 14, 2014Assignee: SanofiInventors: Zhongli Gao, Daniel Hall, David Stefany