The Additional Hetero Ring Consists Of One Oxygen And Four Carbons Patents (Class 546/214)
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Aryl and heteroaryl ether derivatives as liver X receptor beta agonists, compositions, and their use
Patent number: 11655216Abstract: In its many embodiments, the present invention provides certain substituted aryl and heteroaryl ether compounds of the Formula (I): and pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, L, R4, L1, Q, and R5 are as defined herein. The novel compounds of the invention, and pharmaceutically acceptable compositions comprising a compound thereof, are useful as Liver X-? receptor (LXR?) agonists, and may be useful for treating or preventing pathologies related thereto. Such pathologies include, but are not limited to, inflammatory diseases and diseases characterized by defects in cholesterol and lipid metabolism, such as Alzheimer's disease.Type: GrantFiled: October 9, 2017Date of Patent: May 23, 2023Assignee: Merck Sharp & Dohme LLCInventors: Michael T. Rudd, Zhaoyang Meng, Jenny Wai, David Jonathan Bennett, Edward J. Brnardic, Nigel J. Liverton, Shawn J. Stachel, Yongxin Han, Paul Tempest, Jiuxiang Zhu, Xuewang Xu, Bin Zhu -
Patent number: 9018200Abstract: Substituted piperidinyl compounds of the formula (I): are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts are included as well. The compounds are useful as agonists of the g-protein coupled receptor GPR-119.Type: GrantFiled: October 18, 2012Date of Patent: April 28, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Milana Maletic, Harold B. Wood, Wanying Sun
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Publication number: 20150099784Abstract: Novel piperazine, piperidine and tetrahydropyridine derivatives comprising a dibenzofurane moiety are provided herein, as well as pharmaceutical compositions comprising same and therapeutic uses thereof.Type: ApplicationFiled: December 15, 2014Publication date: April 9, 2015Inventors: Vladimir KOGAN, Lev Tabachnik
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Publication number: 20150087675Abstract: Disubstituted 3,4-diamino-3-cyclobutene-1,2-dione compounds corresponding to general formula (I) are disclosed. Also disclosed, are pharmaceutical compositions including these compounds and methods of using these compounds and compositions for the treatment of chemokine-mediated diseases.Type: ApplicationFiled: October 26, 2012Publication date: March 26, 2015Applicant: GLADERMA RESEARCH & DEVELOPMENTInventors: Branislav Musicki, Jerôme Aubert, Patricia Rossio, Marlène Schuppli-Nollet, Laurence Clary, Jean-Guy Boiteau
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Patent number: 8987248Abstract: The invention relates to novel substituted piperidines, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular of cardiovascular disorders and tumor disorders.Type: GrantFiled: March 12, 2010Date of Patent: March 24, 2015Assignee: Bayer Intellectual Property GmbHInventors: Mario Jeske, Dirk Heimbach, Susanne Röhrig, Yolanda Cancho Grande, Dirk Schneider, Ulrich Rester, Eckhard Bender, Mark Meininghaus, Katja Zimmermann, Dmitry Zubov, Anja Buchmüller, Georges Von Degenfeld, Christoph Gerdes, Michael Gerisch, Mark Jean Gnoth, Kersten Matthias Gericke
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Publication number: 20150079520Abstract: An acid diffusion control agent includes a compound represented by a formula (1), a compound represented by a formula (2) or both thereof. R1 represents a hydrocarbon group comprising a monovalent alicyclic structure, or the like. R2 and R3 each independently represent a monovalent hydrocarbon group, or the like. R4 and R5 each independently represent a monovalent hydrocarbon group, or the like. R6 and R7 each independently represent a monovalent hydrocarbon group, or the like. R8 represents a monocyclic heterocyclic group together with the ester group and with the carbon atom. n is an integer of 1 to 6. R9 represents a monovalent hydrocarbon group, or the like. R10 represents a monovalent hydrocarbon group having 1 to 10 carbon atoms. R11 and R12 each independently represent a monovalent hydrocarbon group, or the like. R13 and R14 each independently represent a monovalent hydrocarbon group, or the like.Type: ApplicationFiled: November 14, 2014Publication date: March 19, 2015Applicant: JSR CORPORATIONInventors: Hayato NAMAI, Norihiko IKEDA
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Publication number: 20150080349Abstract: The present invention provides compounds and methods for modulation of the quorum sensing of bacteria. In an embodiment, the compounds of the present invention are able to act as replacements for naturally occurring bacterial quorum sensing ligands in a ligand-protein binding system; that is, they imitate the effect of natural ligands and produce an agonistic effect. In another embodiment, the compounds of the present invention are able to act in a manner which disturbs or inhibits the naturally occurring ligand-protein binding system in quorum sensing bacteria; that is, they produce an antagonistic effect. The compounds of the present invention comprise N-acylated-homoserine lactones (AHLs) comprised of a wide range of acyl groups.Type: ApplicationFiled: July 10, 2014Publication date: March 19, 2015Inventors: Helen E. BLACKWELL, Grant D. GESKE, Jennifer C. CAMPBELL
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Publication number: 20150045367Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of histone deacetylase 8 (HDAC8). Also described herein are methods of using such HDAC8 inhibitors, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of HDAC8 activity.Type: ApplicationFiled: December 19, 2012Publication date: February 12, 2015Inventors: Erik Verner, Wei Chen, Sriram Balasubramanian
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Patent number: 8895551Abstract: The invention relates to acrylamide compounds of Formula I mentioned below. The invention is also directed to the use compounds of Formula I to treat or prevent a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.Type: GrantFiled: April 2, 2010Date of Patent: November 25, 2014Assignee: Shionogi & Co., Ltd.Inventors: Hidenori Mikamiyama, Akira Matsumura, Moriyasu Masui, Kosuke Anan, Kayoko Hata
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Publication number: 20140296202Abstract: Substituted piperidinyl compounds of the formula (I): are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts are included as well. The compounds are useful as agonists of the g-protein coupled receptor GPR-119.Type: ApplicationFiled: October 18, 2012Publication date: October 2, 2014Applicant: Merck Sharp & Dohme Corp.Inventors: Milana Maletic, Harold B. Wood, Wanying Sun
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Publication number: 20140235628Abstract: This invention relates to compounds having structural Formula I: and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds of Formula I are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.Type: ApplicationFiled: September 10, 2012Publication date: August 21, 2014Inventors: Shawn Walsh, Alexander Pasternak, Brian Cato, Paul E. Finke, Jessica Frie, Qinghong Fu, Dooseop Kim, Barbara Pio, Aurash Shahripour, Zhi-Cai Shi, Haifeng Tang
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Publication number: 20140228375Abstract: The present invention involves new and original sigma receptors ligands: (Mono-or dialkylaminoalkyl)-?-butyrolactones, their analogues aminotetrahydroturanes, the (1-adamantyl) benzene alkylamines, the N,N Dialkyl ?-[(adamantyl-1)benzyloxy-2] alkylamines and the 3-cyclopentyl adamantyl-amines or alkylamines or-alkyl phenylamines, their enantiomers or diastereoisomers, their pharmaceutically acceptable salts and Quinacrine Me-thylene blue, Asteinizole and their relative analogues with pro-apoptotic and/or anti-apoptotic properties over cellular biochemical mechanisms, with prototypical anti-cancer, antimetastatic and antiviral activities associated with antagonism of the neuropatic pain and, at very low doses, with cytoprotective and cytoregenerative activity against the cytodegenerative diseases.Type: ApplicationFiled: March 12, 2014Publication date: August 14, 2014Applicant: Anavex Life Sciences Corp.Inventor: Alexandre Vamvakides
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Publication number: 20140221428Abstract: Provided herein are arylsulfonamides that are useful for modulating CCR3 activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition.Type: ApplicationFiled: April 22, 2014Publication date: August 7, 2014Applicant: Axikin Pharmaceuticals, Inc.Inventors: Tai Wei LY, Garrett Thomas POTTER, Jared Andrew FORRESTER
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Patent number: 8741894Abstract: Provided herein are arylsulfonamides that are useful for modulating CCR3 activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition.Type: GrantFiled: March 17, 2011Date of Patent: June 3, 2014Assignee: Axikin Pharmaceuticals, Inc.Inventors: Tai Wei Ly, Garrett Thomas Potter, Jared Andrew Forrester
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Patent number: 8697332Abstract: An object of the present invention is to provide a base generator which has sensitivity and is applicable to a wide range of applications, and a photosensitive resin composition which is applicable to a wide range of applications due to the structure of a polymer precursor in which reaction into a final product is promoted by a basic substance or by heating in the presence of a basic substance. The base generator generates a base by exposure to electromagnetic radiation and heating. The photosensitive resin composition comprises a polymer precursor in which reaction into a final product is promoted by the base generator and a basic substance or by heating in the presence of a basic substance.Type: GrantFiled: March 26, 2010Date of Patent: April 15, 2014Assignee: Dai Nippon Printing Co., Ltd.Inventors: Mami Katayama, Shunji Fukuda, Katsuya Sakayori, Kouji Kawaguchi
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Patent number: 8691848Abstract: The present invention relates to novel classes of compounds which are caspase inhibitors, in particular interleukin-1? converting enzyme (“ICE”) inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting caspase activity and consequently, may be advantageously used as agents against interleukin-1-(“IL-1”), apoptosis-, interferon-? inducing factor-(IGIF), or interferon-?-(“IFN-?”) mediated diseases, including inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, and degenerative diseases. This invention also relates to methods for inhibiting caspase activity and decreasing IGIF production and IFN-? production and methods for treating interleukin-1, apoptosis-, and interferon-?-mediated diseases using the compounds and compositions of this invention.Type: GrantFiled: January 22, 2008Date of Patent: April 8, 2014Assignee: Vertex Pharmaceuticals IncorporatedInventors: Marion W. Wannamaker, Guy W. Bemis, Paul S. Charifson, David J. Lauffer, Michael D. Mullican, Mark A. Murcko, Keith P. Wilson, James W. Janetka, Robert J. Davies, Anne-Laure Grillot, Zhan Shi, Cornelia J. Forster
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Patent number: 8686152Abstract: The present invention is directed to 4,4-di-substituted piperidine derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by DPP-1.Type: GrantFiled: March 9, 2011Date of Patent: April 1, 2014Assignee: Janssen Pharmaceutica NVInventors: Bart L. DeCorte, Renee L. DesJarlais, Yifang Huang, Michael H. Parker, Dennis J. Hlasta
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Publication number: 20140088077Abstract: The invention relates to substituted tetrahydronaphthalenes and derivatives thereof, and also to the physiologically compatible salts and physiologically functional derivatives thereof, to preparation thereof, to medicaments comprising at least one inventive substituted tetrahydronaphthalene or derivative thereof, and to the use of the inventive substituted tetrahydronaphthalenes and derivatives thereof as medicaments.Type: ApplicationFiled: December 3, 2013Publication date: March 27, 2014Applicant: SANOFIInventors: Lothar Schwink, Siegfried Stengelin, Matthias Gossel, Torsten Haack, Petra Lennig
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Patent number: 8674100Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are as set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. The compounds of formula I are useful for treating a variety of disorders including autoimmune diseases such as rheumatoid arthritis, multiple sclerosis and psoriasis.Type: GrantFiled: April 18, 2007Date of Patent: March 18, 2014Assignee: Janssen Pharmaceutica, N.V.Inventors: Carl R. Illig, Shelley K. Ballentine, Jinsheng Chen, Renee Louise DesJariais, Sanath K. Meegalla, Mark Wall, Kenneth Wilson
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Publication number: 20140073627Abstract: The invention relates to compounds of formula (I) wherein R1, R1a, R1b, R2, R3 and X, X1, X2, X3 have the meaning as cited in the description and the claims. Said compounds are useful as Bradykinin B1 antagonists. The invention also relates to pharmaceutical compositions, the preparation of such compounds as well as the production and use as medicament.Type: ApplicationFiled: November 7, 2013Publication date: March 13, 2014Applicant: EVOTEC AGInventors: James MADDEN, David James HALLETT, Alastair PARKES, Ali RAOOF, Xiaolu WANG
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Publication number: 20140058021Abstract: A composition, which comprises a) an organic material susceptible to oxidative, thermal or light-induced degradation; and b) a compound of formula I (Formula I) (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are independently from each other H, C1-C8-alkyl, C4-C8-cycloalkyl, phenyl, C1-C4-alkoxy or halogen; n is 1, 2, 3, or 4; and when n is 1 A is —C(=0)-OR?1, —C(=0)-N(R?2)(R?3), —CN, phenyl, which is unsubstituted or substituted by one or more C1-C8-alkyl, C4-C8-alkoxy, C5-C7-cycloalkyl or halogen, —H or —S02-phenyl; when n is 2 A is —C(=0)-O—Z1—O—C(=0)-, —C(=0)-N(R?1)—Z2—N(R?2)—C(=0)- or piperazine-N,N?-biscarbonyl.Type: ApplicationFiled: April 25, 2012Publication date: February 27, 2014Applicant: BASF SEInventors: Walter Fischer, Abdel-Ilah Basbas, Kai-Uwe Schoning, Cinzia Tartarini, Werner Holzl, Bruno Rotzinger
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Publication number: 20140011845Abstract: Disclosed are cyclic dione derivatives represented by formula (I), wherein the substituents are as defined in the description. The preparation method, intermediate and use thereof are also provided.Type: ApplicationFiled: December 30, 2011Publication date: January 9, 2014Applicant: SYNGENTA PARTICIPATIONS AGInventors: Stephane Andre Marie Jeanmart, Long Lu, Yaming Wu, Lisheng Mao, Michel Muehlbeach
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Patent number: 8614211Abstract: Chemical entities that are arctigenin derivatives, pharmaceutical compositions and methods of treatment of cancer are described.Type: GrantFiled: August 10, 2012Date of Patent: December 24, 2013Assignee: NeuPharma, Inc.Inventors: Xiangping Qian, Yong-Liang Zhu
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Publication number: 20130274288Abstract: The invention provides compounds of formula I: wherein a, b, c, m, n, q, r, W, Z1, Ar1, Z2, Y, R1, R2, and R3 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.Type: ApplicationFiled: June 11, 2013Publication date: October 17, 2013Applicant: THERAVANCE, INC.Inventors: YongQi Mu, Yu-Hua Ji, Mathai Mammen, Viengkham Malathong
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Publication number: 20130261155Abstract: The present invention relates to fungicidal 1-(heterocyclic carbonyl) piperidines and their thiocarbonyl derivatives, their process of preparation and intermediate compounds for their preparation, their use as fungicides, particularly in the form of fungicidal compositions and methods for the control of phytopathogenic fungi of plants using these compounds or their compositions.Type: ApplicationFiled: October 20, 2011Publication date: October 3, 2013Inventors: Jurgen Benting, Peter Dahmen, Philippe Desbordes, Stephanie Gary, Jean-Pierre Vors, Ulrike Wachendorff-Neumann
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Patent number: 8546588Abstract: This invention provides compounds of formula (I): wherein X1, X2, X3, R2, R4b, R1, and G have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.Type: GrantFiled: February 25, 2011Date of Patent: October 1, 2013Assignee: Millennium Pharmaceuticals, Inc.Inventors: Christopher Blackburn, Kenneth M. Gigstad, He Xu
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Patent number: 8519137Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: GrantFiled: October 10, 2008Date of Patent: August 27, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Pramod Joshi, Paul Krenitsky, Andreas Termin, Dean Wilson
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Publication number: 20130210625Abstract: Compounds of the formula (I), wherein the substituents are as defined in claim 1, are useful as a pesticides.Type: ApplicationFiled: May 19, 2011Publication date: August 15, 2013Applicant: SYNGENTA CROP PROTECTION LLCInventors: Michel Muehlebach, Jurgen Harry Schaetzer
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Patent number: 8501782Abstract: The present application describes modulators of MIP-1? of formula (I) or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein m, Q, T, W, Z, R1, R3, R4, R5, R5a and R5b, are as defined herein. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis using the modulators of formula (I) are disclosed.Type: GrantFiled: July 23, 2008Date of Patent: August 6, 2013Assignee: Bristol-Myers Squibb CompanyInventors: Daniel S. Gardner, John V. Duncia, John Hynes, T.G. Murali Dhar, Percy H. Carter, Joseph B. Santella
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Publication number: 20130085127Abstract: A heterocyclic compound useful as an antiallergic agent is provided. A compound represented by the following formula (1) or a salt thereof: wherein the ring A is a homocyclic or heterocyclic ring; the ring B is a heterocyclic ring which contains G and nitrogen atom N as constituent atoms thereof, wherein G is CH or N; R1 is a carbonyl group or an alkylene group; R2a and R2b are an alkyl group, a cycloalkyl group, an aryl group, or a heterocyclic group; X is an oxygen atom or a sulfur atom; Z is a hydroxyl group, an alkoxy group, a cycloalkyloxy group, an aryloxy group, an aralkyloxy group, an amino group, or an N-substituted amino group; and n is 0 or 1; with the proviso that when the ring A is a benzene ring or when the ring B is a piperazine ring, R1 is an alkylene group which may have a substituent.Type: ApplicationFiled: May 23, 2011Publication date: April 4, 2013Applicant: ASKA Pharmaceutical Co., LtdInventors: Makoto Okada, Koichi Hasumi, Takahiro Nishimoto, Miwa Yoshida, Kouki Ishitani, Tomoji Aotsuka, Hashime Kanazawa
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Patent number: 8410138Abstract: Compositions and methods for treatment and prevention of disorders and conditions characterized by reduced TGF-? signaling are described.Type: GrantFiled: December 12, 2011Date of Patent: April 2, 2013Assignees: The Board of Trustees of the Leland Stanford Junior University, SRI InternationalInventors: Anton Wyss-Coray, Mary J. Tanga
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Patent number: 8404693Abstract: 3,4-Disubstituted-4-aryl-piperidine compounds are disclosed. Pharmaceutical compositions containing the 3,4-disubstituted-4-aryl-piperidine compounds and methods of their pharmaceutical uses are also disclosed. The compounds disclosed are useful, inter alia, as antagonists of opioid receptors.Type: GrantFiled: January 17, 2011Date of Patent: March 26, 2013Assignee: Adolor CorporationInventors: Roland E. Dolle, Bertrand Le Bourdonnec
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Publication number: 20130053364Abstract: The invention provides sulphone compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making various sulphone compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2.Type: ApplicationFiled: April 23, 2012Publication date: February 28, 2013Inventors: Hazel J. Dyke, Susan M. Cramp, Thomas D. Pallin, Janusz J. Kulagowski, John G. Montana, Robert Zahler
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Publication number: 20130053385Abstract: The use of a compound of formula I wherein the substituents are as defined in claim 1, or compositions containing them in controlling insects, acarines, nematodes or molluscs.Type: ApplicationFiled: December 7, 2010Publication date: February 28, 2013Applicants: SYNGENTA LIMITED, SYNGENTA CROP PROTECTION LLCInventors: Stephane Andre Marie Jeanmart, Russell Viner, John Benjamin Taylor, William Guy Whittingham, Jeffrey Steven Wailes, Sarah Margaret Targett, Christopher John Mathews, Michel Muehlebach
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Patent number: 8383821Abstract: The invention encompasses compounds of Formula I, including pharmaceutically acceptable salts, their pharmaceutical compositions, and their use in treating disorders associated with an excess or imbalance of tachykinins or serotonin or both.Type: GrantFiled: November 13, 2009Date of Patent: February 26, 2013Assignee: Bristol-Meyers Squibb CompanyInventors: Andrew P. Degnan, Kevin W. Gillman, Derek J. Denhart, Jonathan L. Ditta, Ramkumar Rajamani, Ying Han, George O. Tora
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Publication number: 20130040945Abstract: Chemical entities that are arctigenin derivatives, pharmaceutical compositions and methods of treatment of cancer are described.Type: ApplicationFiled: August 10, 2012Publication date: February 14, 2013Inventors: Xiangping Qian, Yong-Liang Zhu
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Publication number: 20120302539Abstract: Certain compounds and pharmaceutically acceptable salts are provided herein. Also provided are pharmaceutical compositions comprising at least one compound or pharmaceutically acceptable salt therein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain disease states responsive to the inhibition of transglutaminase TG2 activity are described. These disease states include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound or pharmaceutically acceptable salt thereof as a single active agent or administering at least one compound or pharmaceutically acceptable salt thereof in combination with one or more other therapeutic agents.Type: ApplicationFiled: May 7, 2012Publication date: November 29, 2012Inventors: Michael Prime, Stephen Martin Courtney, Richard Marston, Celia Dominguez, Douglas Macdonald, John Wityak
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Publication number: 20120283222Abstract: Compounds represented by formula (I): wherein each symbol is as defined in the description, and pharmaceutically acceptable salts thereof are useful as hyperglycemic inhibitors having a serine protease inhibitory action and as prophylactic or therapeutic drugs for diabetes.Type: ApplicationFiled: May 31, 2012Publication date: November 8, 2012Applicant: Ajinomoto Co., Inc.Inventors: Atsushi KONISHI, Munetaka Tokumasu, Tamotsu Suzuki, Takahiro Koshiba, Koji Ohsumi, Osamu Ikehara, Yuko Kodama
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Publication number: 20120238574Abstract: The present invention relates to (1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl derivatives having the general formula (I) to pharmaceutical compositions comprising the same and to the use of these (1,1,1,3,3,3-hexafluoro-2-hydroxy-propan-2-yl)phenyl derivatives in the treatment of atherosclerosis.Type: ApplicationFiled: October 26, 2010Publication date: September 20, 2012Applicant: N.V. ORGANONInventors: Andrew John Cooke, Emma Louise Carswell, David Jonathan Bennett
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Patent number: 8222418Abstract: Compounds of formula I: modulate the action of gamma secretase, and hence find use in treatment of Alzheimer's disease and related conditions.Type: GrantFiled: March 27, 2007Date of Patent: July 17, 2012Assignee: Merck Sharp + Dohme Corp.Inventors: Joanne Clare Hannam, Sascha Hartmann, Andrew Madin, Mark Peter Ridgill
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Patent number: 8211916Abstract: N- and O-substituted 4[2-diaromaticmethoxy and methylamino)alkyl] piperidines exhibit high CNS activity with respect to the dopamine transporter (DAT) and serotonin transporter (SERT). Preferred compounds exhibit highly differential behavior as between the DAT and SERT and between the DAT and the norepinephrine transporter (NET). The compounds have utility in treating CNS disorders, including but not limited to cocaine addiction, depression, and Parkinson's disease.Type: GrantFiled: January 22, 2008Date of Patent: July 3, 2012Assignee: Wayne State UniversityInventor: Aloke K. Dutta
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Patent number: 8207345Abstract: Compounds of the formula (I), in which W, R, R1, R2, R3, R4, R5, R6 and R7 have the meanings indicated in Claim 1, can be employed, inter alia, for the treatment of tumors.Type: GrantFiled: June 2, 2006Date of Patent: June 26, 2012Assignee: Merck Patent GmbHInventors: Kai Schiemann, David Bruge, Hans-Peter Buchstaller, Ulrich Emde, Dirk Finsinger, Christiane Amendt, Frank Zenke
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Patent number: 8198304Abstract: The invention provides compounds of formula I: or a pharmaceutically acceptable salt thereof, wherein R1-3, R5-7, a, X, Y, Y?, Y?, and Z are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.Type: GrantFiled: September 9, 2011Date of Patent: June 12, 2012Assignee: Theravance, Inc.Inventors: YuHua Ji, Craig Husfeld, YongQi Mu, Rick Lee, Li Li
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Patent number: 8188288Abstract: The present invention relates to 2-adamantylurea derivatives of formula I as selective inhibitors of the enzyme 11-beta-hydroxysteroid dehydrogenase type 1 (11?-HSD1) and the use of such compounds for the treatment and prevention of metabolic syndrome, diabetes, insulin resistance, obesity, lipid disorders, glaucoma, osteoporosis, cognitive disorders, anxiety, depression, immune disorders, hypertension and other diseases and conditions.Type: GrantFiled: November 22, 2006Date of Patent: May 29, 2012Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Denis Carniato, Christine Charon, Johannes Gleitz, Didier Roche, Bjoern Hock
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Publication number: 20120122926Abstract: The invention provides compounds of formula I: wherein a, b, c, m, n, q, r, W, Z1, Ar1, Z2, Y, R1, R2, and R3 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.Type: ApplicationFiled: January 25, 2012Publication date: May 17, 2012Applicant: THERAVANCE, INC.Inventors: YongQi Mu, Yu-Hua Ji, Mathai Mammen, Viengkham Malathong
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Publication number: 20120122850Abstract: The invention provides compounds of formula I: wherein a, b, c, m, s, t, W, Z, Ar, R1, R2, R3, R6, and R7 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.Type: ApplicationFiled: January 11, 2012Publication date: May 17, 2012Applicant: THERAVANCE, INC.Inventors: Yu-Hua JI, Mathai MAMMEN, Craig HUSFELD, Li LI, YongQi MU, Aaron KUSHNER, Eric STANGELAND, Trevor MISCHKI, Adam HUGHES, Sarah DUNHAM
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Patent number: 8153807Abstract: The present invention discloses novel compounds of Formula I: (I) having 11-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, and other conditions associated with 11-HSD type 1 activity.Type: GrantFiled: April 23, 2007Date of Patent: April 10, 2012Assignee: Eli Lilly and CompanyInventors: Julie Kay Bush, Marvin Martin Hansen, Renhua Li, Thomas Edward Mabry, Nancy June Snyder, Owen Brendan Wallace, Yanping Xu
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Patent number: 8138206Abstract: Disclosed is a substance having an antagonistic effect on the binding of histamine to a histamine H3 receptor or an inhibitory effect on the activity which a histamine H3 receptor constantly exhibits. A compound represented by the formula (I) or a pharmaceutically acceptable salt thereof; (I) wherein R1 represents a phenyl group which may be substituted or the like and R2 represents a cyano group which may be substituted or the like, or R1 and R2 together form an aliphatic heterocylic ring which may be substituted; R3 represents a group represented by the formula (II-1) below; and all of X1 to X4 represent a carbon atom or the like: (II-1) where R4 and R5 represent a lower alkyl group or the like; and m1 represents an integer of 2 to 4.Type: GrantFiled: May 29, 2006Date of Patent: March 20, 2012Assignee: MSD. K.K.Inventors: Shiho Ishikawa, Tsuyoshi Nagase, Nagaaki Sato, Hidekazu Takahashi, Shigeru Tokita, Toshihiro Wada
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Publication number: 20120046268Abstract: The invention relates to novel substituted piperidines, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular of cardiovascular disorders and tumour disorders.Type: ApplicationFiled: March 12, 2010Publication date: February 23, 2012Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Mario Jeske, Dirk Heimbach, Susanne Röhrig, Yolanda Cancho Grande, Dirk Schneider, Ulrich Rester, Eckhard Bender, Mark Meininghaus, Katja Zimmermann, Dmitry Zubov, Anja Buchmüller, Georges Von Degenfeld, Christoph Gerdes, Michael Gerisch, Mark Jean Gnoth, Kersten Matthias Gericke
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Publication number: 20120041019Abstract: Compounds useful as protease inhibitors are provided, as are methods of use and preparation of such compounds and compositions containing such compounds. In one embodiment, the compounds are useful for inhibiting HIV protease enzymes, and are therefore useful in slowing the proliferation of HIV.Type: ApplicationFiled: December 17, 2009Publication date: February 16, 2012Inventors: Mitchell W. Mutz, Kenneth J. Barr, Jason Gestwicki