Unsaturated Carbocyclic Ring Or Acyclic Carbon To Carbon Unsaturation Containing Patents (Class 549/77)
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Patent number: 9108943Abstract: The design, modeling, synthesis, biological evaluation, and photoaffinity labeling studies of a series of photoreactive potent and selective HDACs 1 and 2 benzamide based probes are disclosed herein.Type: GrantFiled: June 18, 2014Date of Patent: August 18, 2015Assignee: THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOISInventor: Pavel Petukhov
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Publication number: 20150065343Abstract: The present invention relates to acrylamide compounds which are useful for combating or controlling invertebrate pests, in particular arthropod pests and nematodes, and to a method for producing them. The invention also relates to a method for controlling invertebrate pests by using these compounds and to plant propagation material and to an agricultural and a veterinary composition comprising said compounds.Type: ApplicationFiled: March 28, 2013Publication date: March 5, 2015Inventors: Pascal Bindschaedler, Wolfgang Von Deyn, Karsten Koerber, Florian Kaiser, Ralph Paulini, Deborah L. Culbertson, Paul Neese, Franz Josef Braun
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Publication number: 20150045398Abstract: The present invention provides a compound of formula (I): said compound is inhibitor of MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12 and/or MMP-13. Accordingly, the compound of formula (I) can be used in treatment of disorders or diseases mediated by MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12, and/or MMP-13. Finally, the present invention also provides a pharmaceutical composition.Type: ApplicationFiled: October 7, 2014Publication date: February 12, 2015Applicant: NOVARTIS AGInventors: Claus EHRHARDT, Leslie Wighton MCQUIRE, Pascal RIGOLLIER, Olivier ROGEL, Michael David SHULTZ, Ruben Alberto TOMMASI
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Publication number: 20140371469Abstract: The design, modeling, synthesis, biological evaluation, and photoaffinity labeling studies of a series of photoreactive potent and selective HDACs 1 and 2 benzamide based probes are disclosed herein.Type: ApplicationFiled: June 18, 2014Publication date: December 18, 2014Inventor: Pavel Petukhov
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Publication number: 20140371291Abstract: A novel serine racemase inhibitor exhibits sufficient activity and specificity. The serine racemase inhibitor includes one or more compounds selected from compounds respectively represented by the following general formulas [MM_1], [DR_1], [DR?_1], [LW_1], and [ED_1] as an active ingredient.Type: ApplicationFiled: January 24, 2013Publication date: December 18, 2014Inventors: Hisashi Mori, Naoki Toyooka, Mineyuki Mizuguchi, Takayuki Obita, Syuichi Hirono, Hiroaki Goda
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Publication number: 20140353553Abstract: A novel compound represented by general formula (1), a carrier system including a carrier having the novel compound fixed thereon, and a photoelectric conversion device having the carrier system. In formula (1), Z is a C1-C50 conjugated group; R1 is a C6-C20 aromatic hydrocarbon group, a C7-C20 aromatic hydrocarbon group substituted by an aliphatic hydrocarbon group, or a C1-C20 aliphatic hydrocarbon group, each substituted by carboxyl, cyano, amino, amide, or nitro, the aliphatic hydrocarbon group being optionally interrupted by —O—, etc.; R2 is hydrogen or an optionally substituted C1-C20 hydrocarbon group; R30, R31, R32, R33, R40, R41, R42, R43, and R44 are each hydrogen or optionally substituted hydrocarbon group, and adjacent two of them may be connected to form a ring; R5 is hydrogen or cyano; and R11 is represented by formula (11-1) or (11-2), wherein n, ring A, and the like are as defined in the description.Type: ApplicationFiled: February 27, 2013Publication date: December 4, 2014Applicant: ADEKA CorporationInventors: Hiroyuki Osada, Yohei Aoyama
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Publication number: 20140323736Abstract: The present application relates to known and novel aryl- and hetarylcarboxamides of the formula (I) and to their use as medicaments for controlling endoparasites in animals or humans, and also to parasiticidal compositions, in particular endoparasites, comprising aryl- and hetarylcyclylcarboxamides.Type: ApplicationFiled: November 23, 2012Publication date: October 30, 2014Inventors: Hans-Georg Schwarz, Axel Trautwein, Lothar Willms, Maike Hink, Peter Lummen, Ulrich Gorgens, Pierre-Yves Coqueron, Achim Harder, Claudia Welz
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Publication number: 20140323487Abstract: Novel compounds which are antagonists or inverse agonists at one or more of the opioid receptors, pharmaceutical compositions containing them, to processes for their preparation.Type: ApplicationFiled: July 8, 2014Publication date: October 30, 2014Inventors: David John Cowan, Andrew Lamont Larkin, Cunyu Zhang, David Lee Musso, Gary Martin Green, Rodolfo Cadilla, Paul Kenneth Spearing, Michael Joseph Bishop, Jason Daniel Speake
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Publication number: 20140315965Abstract: The present disclosure relates to novel compounds having vitamin D receptor agonist and histone deacetylase inhibitory efficacy as well as methods for reducing or inhibiting the proliferation of cancer cells or for treating cancer.Type: ApplicationFiled: December 20, 2012Publication date: October 23, 2014Inventors: James L. Gleason, John H. White, Dainis Kaldre, Joshua Fischer
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Patent number: 8865736Abstract: Compounds of formula (I) have antibacterial activity: wherein R represents hydrogen or 1, 2 or 3 optional substituents; W is ?C(R1)—; R1 is hydrogen and R2 is hydrogen, methyl, or fluorine; or R1 and R2 taken together are —CH2—, —CH2CH2, —O—, or, in either orientation, —O—CH2— or —OCH2CH2—; and R3 is a radical of formula -(Alk1)m-(Z)p-(Alk2)n-Q.Type: GrantFiled: November 28, 2011Date of Patent: October 21, 2014Assignee: Biota Scientific Pty LtdInventors: David Ryall Brown, Ian Collins, Lloyd George Czaplewski, David John Haydon
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Publication number: 20140303171Abstract: Compounds of Formula I are disclosed: wherein A, R1, R2, R3, R4A, R4B, R5, R6 and R7 are defined herein. The compounds encompassed by Formula I include compounds which are HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: ApplicationFiled: October 26, 2012Publication date: October 9, 2014Inventors: Michael John Boyd, Jean-Francois Chiasson, Sheldon Crane, André Giroux
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Publication number: 20140290748Abstract: The present invention relates to an organic colorant corresponding to one of the following structures (I) or (II): eD-pi-conjugated chromophore-L-A??(I) A-L-pi-conjugated chromophore-eD??(II) in which eD represents an electron donor segment; L represents a covalent bond or a spacer segment; A represents an electron attractor segment able to form a covalent bond with a semi-conductor; the pi-conjugated chromophore comprising at least two aromatic rings, at least one of which is a thiophene, selenophene or furan type ring. The present invention relates to the use thereof as photosensitizer in a photovoltaic device and said photovoltaic device.Type: ApplicationFiled: November 12, 2012Publication date: October 2, 2014Applicant: COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVESInventors: Renaud Demadrille, Yann Kervella
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Patent number: 8846955Abstract: Problem to Be Solved: to provide a chromophore having a far superior nonlinear optical activity to conventional chromophores and to provide a nonlinear optical element comprising said chromophore. Solution: a chromophore comprising a donor structure D, a ?-conjugated bridge structure B, and an acceptor structure A, the donor structure D comprising an aryl group substituted with a substituted oxy group; and a nonlinear optical element comprising said chromophore.Type: GrantFiled: August 24, 2010Date of Patent: September 30, 2014Assignees: National Institute of Information and Communications Technology, Sumitomo Electric Industries, Ltd., Kyushu University, National University CorporationInventors: Akira Otomo, Isao Aoki, Hideki Miki, Hidehisa Tazawa, Shiyoshi Yokoyama
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Publication number: 20140275552Abstract: Photoactive compositions of matter, methods for their design and synthesis, and various applications of such compositions of matter are disclosed. Such photoactive compositions may, for example, include any one or more of the following: a core moiety; a primary electron donor moiety; an electron-withdrawing moiety; and an alkyl tail. Some photoactive compositions may further include multiple additional electron donor moieties, electron-withdrawing moieties, and alkyl tails. Applications of such photoactive compositions of matter may include use in photovoltaic cells (e.g., as a p- or n-type material of the active layer of some photovoltaic cells, or as a dye to be employed in other photovoltaic cells); batteries, field-effect transistors; and light-emitting diodes.Type: ApplicationFiled: March 15, 2013Publication date: September 18, 2014Inventors: Michael D. Irwin, Jerred A. Chute, Robert D. Maher, III
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Publication number: 20140249201Abstract: Disclosed are beta and gamma-amino isoquinoline amide compounds and substituted benzamide compounds. In particular, the invention provides compounds that affect the function of kinases in a cell and that are useful as therapeutic agents or with therapeutic agents. The compounds of the invention are useful in the treatment of a variety of diseases and conditions including eye diseases such as glaucoma, cardiovascular diseases, and diseases characterized by abnormal growth, such as cancers. The invention further provides compositions containing the beta or gamma-amino isoquinoline amide compounds or substituted benzamide compounds.Type: ApplicationFiled: May 9, 2014Publication date: September 4, 2014Applicant: Aerie Pharmaceuticals, Inc.Inventors: Mitchell A. deLong, Jill Marie Sturdivant, Susan M. Royalty
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Publication number: 20140202537Abstract: Provided is a dye-sensitized solar cell in which the energy conversion efficiency is increased by adsorbing two different kinds of dyes to the surface of titanium oxide that constitutes a semiconductor electrode. In a dye-sensitized solar cell including a conductive support, a porous semiconductor layer having sensitizing dyes adsorbed onto this conductive support, a carrier transport layer and a counter electrode, the energy conversion efficiency is increased by adsorbing a mixture of a ruthenium complex, and an organic dye having a different molecular size and exhibiting a high open circuit voltage as a photoelectric conversion characteristic obtainable by the dye alone, onto the porous semiconductor layer.Type: ApplicationFiled: August 24, 2012Publication date: July 24, 2014Inventors: Liyuan Han, Ashraful Islam
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Publication number: 20140206741Abstract: The present invention provides an N-substituted isopropyldimethyl azulene sulfonamide derivative as represented by formula (I), and preparation method and uses thereof, wherein R1 is an alkyl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, amino, or a substituted alkyl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, and amino. The N-substituted isopropyldimethyl azulene sulfonamide derivative can be used in treating gastric ulcer.Type: ApplicationFiled: April 12, 2012Publication date: July 24, 2014Applicant: Sichuan Guokang Pharmaceutical Co., LtdInventors: Luyun Zhang, Fang Yang, Wanqi Shi, Ping Zhang, Ying Li, Shufan Yin
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Patent number: 8772296Abstract: Benzamide derivatives of formula I are described and have therapeutic utility, particularly in the treatment of diabetes, obesity and related conditions and disorders: wherein R1, R2, R3, R4, R5, R6, R7, R8, and n are as defined herein.Type: GrantFiled: May 31, 2007Date of Patent: July 8, 2014Assignee: Amgen Inc.Inventors: Jay P. Powers, Michael Degraffenreid, Lisa Julian, Jacob Kaizerman, Dustin McMinn, Yosup Rew, Daqing Sun, Xuelei Yan, Zhulun Wang, Felix Gonzalez Lopez De Turiso
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Patent number: 8759388Abstract: Disclosed are beta and gamma-amino isoquinoline amide compounds and substituted benzamide compounds. In particular, the invention provides compounds that affect the function of kinases in a cell and that are useful as therapeutic agents or with therapeutic agents. The compounds of the invention are useful in the treatment of a variety of diseases and conditions including eye diseases such as glaucoma, cardiovascular diseases, and diseases characterized by abnormal growth, such as cancers. The invention further provides compositions containing the beta or gamma-amino isoquinoline amide compounds or substituted benzamide compounds.Type: GrantFiled: April 9, 2012Date of Patent: June 24, 2014Assignee: Aerie Pharmaceuticals, Inc.Inventors: Mitchell A. deLong, Jill Marie Sturdivant, Susan M. Royalty
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Patent number: 8741951Abstract: The present invention concerns compounds of general Formula (I): method of preparation and uses thereof.Type: GrantFiled: April 12, 2010Date of Patent: June 3, 2014Assignees: CNR—Consiglio Nazionale delle Ricerche, Istituto Scientifico Romagnolo per lo Studio e la Cura dei Tumori (I.R.S.T.) S.r.l.Inventors: Greta Varchi, Andrea Guerrini, Anna Tesei, Giovanni Brigliadori
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Patent number: 8729532Abstract: The present invention provides a light-absorbing material capable of providing high photoelectric conversion efficiency when applied to a photoelectric conversion element. The light-absorbing material of the present invention has a structure represented by Formula (1) below: X—Y??(1) (wherein X represents a light-absorbing site, and Y represents a radical site that becomes a radical when in an oxidized state and/or when in a reduced state, and is capable of repeated oxidation-reduction).Type: GrantFiled: May 21, 2010Date of Patent: May 20, 2014Assignees: Panasonic Corporation, Waseda UniversityInventors: Takashi Sekiguchi, Hiroyuki Nishide, Michio Suzuka, Takeyuki Yamaki, Kenichi Oyaizu, Fumiaki Kato, Satoko Kambe
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Publication number: 20140088046Abstract: The present invention provides novel phenicol derivatives, their use for the treatment of infections in mammals, pharmaceutical composition containing these novel compounds, and methods for the preparation of these compounds.Type: ApplicationFiled: September 5, 2013Publication date: March 27, 2014Applicant: ZOETIS LLCInventors: Denis Billen, Michael Curtis, Richard Andrew Ewin, Richard M. Goodwin, Paul D. Johnson, Timothy Allan Johnson, Graham M. Kyne, Todd M. Maddux, Susan Mary Kult Sheehan, Rajendran Vairagoundar
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Patent number: 8680336Abstract: Dyes for dye-sensitized solar cell are provided. Each of the dyes for a dye-sensitized solar cell according to an embodiment has a chemical structure: wherein each of X and Y may comprise a substituent, comprising aromatic hydrocarbon groups which are respectively independently substituted or unsubstituted, aromatic heterocyclic groups which are substituted or unsubstituted, and a combination thereof, Z may comprise aromatic hydrocarbon groups which are substituted or unsubstituted, heterocyclic groups which are substituted or unsubstituted, vinyl groups, and polyvinyl groups which are substituted or unsubstituted, and A may comprise acid functional groups.Type: GrantFiled: September 16, 2009Date of Patent: March 25, 2014Assignee: LG Display Co., Ltd.Inventors: Jonghyun Park, Seongkee Park, Sunghoon Joo, Jinok Hwang, Taeyoun Kim
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Publication number: 20140081017Abstract: The present invention relates to compositions and methods to selectively treat fungal infection. More particularly, the invention relates to compounds, compositions thereof, and methods for selectively enhancing fungal sensitivity to antifungal compounds.Type: ApplicationFiled: March 14, 2013Publication date: March 20, 2014Applicant: METHYLGENE INC.Inventor: METHYLGENE INC.
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Publication number: 20140080832Abstract: Compounds which directly inhibit IRE-1? activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response and can be used as single agents or in combination therapies.Type: ApplicationFiled: November 13, 2013Publication date: March 20, 2014Applicant: MANNKIND CORPORATIONInventors: John Bruce PATTERSON, David Gregory LONERGAN, Gary A. FLYNN, Qingping ZENG, Peter V. PALLAI
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Publication number: 20140080800Abstract: The present invention relates to compounds of formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, wherein U, J, V, X, R2a, R2b, R2c, R5 and t are as described herein. The present invention relates generally to inhibitors of histone deacetylase and to methods of making and using them. These compounds are useful for promoting cognitive function and enhancing learning and memory formation. In addition, these compounds are useful for treating, alleviating, and/or preventing various conditions, including for example, neurological disorders, memory and cognitive function disorders/impairments, extinction learning disorders, fungal diseases and infections, inflammatory diseases, hematological diseases, and neoplastic diseases in humans and animals.Type: ApplicationFiled: October 28, 2013Publication date: March 20, 2014Inventors: Edward Holson, Florence Fevrier Wagner, Michel Weiwer, Li-Huei Tsai, Stephen Haggarty, Yan-Ling Zhang
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Patent number: 8653279Abstract: The present embodiments relate to a dye for a dye-sensitized solar cell and a dye-sensitized solar cell prepared from the same. The dye includes a fluorenyl-containing compound. The dye according to the present embodiments is applied to a light absorption layer to improve photovoltaic efficiency and increase an open-circuit voltage.Type: GrantFiled: April 16, 2007Date of Patent: February 18, 2014Assignee: Samsung SDI Co., Ltd.Inventors: Jae-Kwan Lee, Ji-Won Lee, Jae-Jung Ko, Sang-Hoon Kim, Soo-Jin Moon, Moon-Sung Kang, Moon-Seok Kwon
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Patent number: 8652752Abstract: Compounds of the Formula (I), wherein L1, L?1, L?1, L2, L?2, L?2, L3, L?3, L?3, L4, L?4 and L?4 for example are hydrogen or COT; R, R? and R? for example are hydrogen, C6-C12aryl or C3-C20heteroaryl; X, X? and X? for example are O, S, single bond, NRa or NCORa, T is for example hydrogen, C1-C20alkyl, C3-C12cycloalkyl, C2-C20alkenyl, C5-C12cycloalkenyl, C7-C18cycloalkylenaryl, C5-C18cycloalkylenheteroaryl, C6-C14aryl, providedthat at least one of R, R? or R? is unsubstituted or substituted C3-C20heteroaryl; and Y is an inorganic or organic anion; are suitable as photolatent acid generators.Type: GrantFiled: September 22, 2008Date of Patent: February 18, 2014Assignee: BASF SEInventors: Pascal Hayoz, Hitoshi Yamato, Toshikage Asakura
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Publication number: 20140018377Abstract: This application claims priority to European Patent Application No. 09173304.8, filed Oct. 16, 2009, and the benefit of U.S. Provisional Application No. 61/253,091, filed Oct. 20, 2009, the disclosure of each of which is incorporated by reference herein in its entirety. The present invention relates to aminopropenoate derivatives, the process of their preparation, intermediate compounds, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants and in material protection, using these compounds or compositions.Type: ApplicationFiled: June 12, 2013Publication date: January 16, 2014Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Christophe Dubost, Jacky Vadal, Philippe Rinolfi, Marie-Claire Grosjean-Cournoyer, Mazen Es-Sayed, Jürgen Benting, Ulrike Wachendorff-Neumann, Shinichi Narabu, Koichi Ishikawa, Hiroyuki Hadano, Pierre Genix, Jean-Pierre Vors, Angela Becker, Ulrich Görgens
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Patent number: 8614337Abstract: The chiral compound S-5-substituted-N-2?-(thienyl-2-yl-)ethyl-tetralin-2-amine or its chiral acid salts and preparation method thereof are disclosed, and the method for preparing Rotigotine by using the chiral compound is also disclosed. Racemic 5-substituted-N-2?-(thien-2-yl-)ethyl-tetralin-2-amine (compound 1) is resolved by using a conventional chiral acid to obtain an optically pure chiral acid salt of S-5-substituted-N-2?-(thien-2-yl-)ethyl-tetralin-2-amine, which is then dissociated to obtain S-5-substituted-N-2?-(thien-2-yl-)ethyl-tetralin-2-amine (compound 2). The compound 2 or chiral acid salt thereof is alkylated and deprotected to produce rotigotine (compound 5).Type: GrantFiled: September 7, 2010Date of Patent: December 24, 2013Assignee: 2Y-Chem Ltd.Inventors: Xungui He, Jianping Guo, Yanling Wang, Wensheng Tang, Xingzhong Zhang, Xuezhang Wang, Yuan Wang
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Publication number: 20130337382Abstract: A compound represented by general formula (b1) shown below (in the formula, Y1 represents a divalent linking group; W represents S, Se or I; R1 represents a hydrocarbon group; represents an alkyl group of 1 to 5 carbon atoms or an alkoxy group of 1 to 5 carbon atoms; when W represents I, m+n=2, and when W represents S or Se, m+n=3, provided that m?1 and n?0; p represents an integer of 0 to 5; and X? represents a counteranion.Type: ApplicationFiled: June 11, 2013Publication date: December 19, 2013Inventors: Yoshiyuki Utsumi, Hideto Nito
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Publication number: 20130324557Abstract: The present invention includes compounds useful as modulators of TRPM8, such as compounds of Formula (I) and the subgenus and species thereof; personal products containing those compounds; and the use of those compounds and the personal products, particularly the use of increasing or inducing chemesthetic sensations, such as cooling or cold sensations.Type: ApplicationFiled: November 4, 2011Publication date: December 5, 2013Applicant: SENOMYX, INC.Inventors: Chad Priest, Alain Noncovich, Andrew Patron, Jane Ung
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Publication number: 20130317078Abstract: The method of treating patients by administering N-[3-[5-[(4-fluorophenyl)methyl]-2-thienyl]-1-methyl-2-propynyl]-N-hydroxyurea for treatment of leukotriene related pathologies, and compositions for this use.Type: ApplicationFiled: June 20, 2013Publication date: November 28, 2013Inventors: Rebecca Taub, Tilmann Brotz, John Franc, Lawrence K. Cohen, Hemantkumar H. Patel, Sanjay R. Chemburkar, David P. Sawick
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Publication number: 20130310559Abstract: Among other things, the present invention provides novel isoprenyl compounds capable of effectively modulating inflammatory responses and pharmaceutical, cosmetic, cosmeceutical and topical compositions comprising these isoprenyl compounds. Anti-inflammatory compounds of the present invention are useful in treating or preventing diseases or conditions associated with inflammation. Proinflammatory compounds of the present invention are useful in treating or preventing diseases or conditions associated with suppression of inflammatory responses. Thus, the present invention also provides methods useful in the treatment or prevention of diseases or conditions associated with inflammation as well as methods useful in the treatment or prevention of diseases or conditions associated with suppression of inflammatory responses.Type: ApplicationFiled: February 6, 2013Publication date: November 21, 2013Applicant: SIGNUM BIOSCIENCES, INC.Inventors: Jeffry B. Stock, Maxwell Stock, Keshava Rapole, Seung-Yub Lee, Michael Voronkov, Eduardo Perez, Joel Gordon, Shuyi Chen, Jinglong Chen
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Patent number: 8586603Abstract: The present application relates to compounds of formula (I): and pharmaceutically acceptable salts and solvates thereof, wherein the substituents are as defined herein, compositions containing such compounds and the uses of such compounds in producing medicaments for the treatment of various diseases and conditions, such as of the central nervous system.Type: GrantFiled: December 20, 2010Date of Patent: November 19, 2013Inventors: Peter Gmeiner, Miriam Ruberg, Harald Hüebner
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Publication number: 20130303549Abstract: Novel biaromatic compounds having the general formula (I): and cosmetic/pharmaceutical compositions comprised thereof are useful in human or veterinary medicine (in dermatology and also in the fields of cardiovascular diseases, of immune diseases and/of diseases related to the metabolism of lipids), or, alternatively, in cosmetic compositions.Type: ApplicationFiled: July 10, 2013Publication date: November 14, 2013Inventors: Jean-Guy BOITEAU, Laurence CLARY, Corinne Millois BARBUIS
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Publication number: 20130281705Abstract: Compounds useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis, are disclosed.Type: ApplicationFiled: June 18, 2013Publication date: October 24, 2013Inventor: Shalini SHARMA
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Publication number: 20130281453Abstract: Serine hydrolases are implicated in malconditions such as cancer, central nervous system disorders, cardiovascular disorders, obesity, and metabolic disorders. Many serine hydrolases expressed in proteomic libraries are of unknown function in vivo. Compounds identified through library versus library screening can be used for treatment of malconditions associated with the specific serine hydrolase KIAA1363 (also known as AADACL1). A library of inhibitors of KIAA1363 was prepared and candidate compounds were identified as a potent inhibitors having submicromolar IC50 values. An exemplary compound of the invention was shown to be an effective inhibitor of prostate cancer pathogenesis. Other inhibitory compounds of the invention comprising fluorophore groups are shown to be effective in spatial and temporal localization of the serine hydrolase in cells and tissues.Type: ApplicationFiled: October 21, 2011Publication date: October 24, 2013Applicant: The Scripps Research InstituteInventors: Benjamin Cravatt, Daniel Nomura, Jae W. Chang, Raymond E. Moellering, Dan Bachovehin, Weiwei Li
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Patent number: 8536300Abstract: Photocrosslinkable electrically conductive polymers and compositions including the polymers are provided. Also, electrically conductive layers or films formed from the compositions, preparation methods of these, and articles including the electrically conductive layers or films are provided. The electrically conductive polymers according to the present disclosure have photoreactive groups that can be crosslinked using like. The electrically conductive polymers can also be dissolved in aqueous solution. These photocrosslinkable and soluble properties allow the electrically conductive polymers to be used in wet processing to make films and/or to be made into a patterned conductive layer or film using a photomask.Type: GrantFiled: December 30, 2009Date of Patent: September 17, 2013Assignee: Korea University Research and Business FoundationInventor: Dong Hoon Choi
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Publication number: 20130231479Abstract: The present invention provides a pest control agent, acaricide or fungicide that contains, as the active ingredient thereof, at least one type of compound selected from the aryloxyurea compounds represented by formula (V) (wherein R1 to R5 each independently represents an alkyl group or the like, X is a halogen atom or the like, n is an integer of 0 to 5, and Z is an oxygen atom or sulfur atom) or salts thereof.Type: ApplicationFiled: October 6, 2011Publication date: September 5, 2013Inventors: Hironori Furukawa, Takehiko Nakamura, Tetsuo Tamai, Daisuke Hanai
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Publication number: 20130217889Abstract: Compounds of formula (I): wherein R1 to R8, and X? are defined herein. Also disclosed are methods of making and using these compounds.Type: ApplicationFiled: October 27, 2011Publication date: August 22, 2013Applicant: National University of SingaporeInventors: Choon Hong Tan, Kuo Wei Huang, Ting Ma, Xiao Fu
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Patent number: 8513297Abstract: Novel biaromatic compounds having the general formula (I): and cosmetic/pharmaceutical compositions comprised thereof are useful in human or veterinary medicine (in dermatology and also in the fields of cardiovascular diseases, of immune diseases and/of diseases related to the metabolism of lipids), or, alternatively, in cosmetic compositions.Type: GrantFiled: January 18, 2012Date of Patent: August 20, 2013Assignee: Galderma Research & DevelopmentInventors: Jean-Guy Boiteau, Laurence Clary, Corinne Millois Barbuis
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Publication number: 20130196978Abstract: Alkaloid aminoester compounds which act as muscarinic receptor antagonists are useful for the prevention and/or treatment of a broncho-obstructive or inflammatory diseases.Type: ApplicationFiled: March 14, 2013Publication date: August 1, 2013Applicant: Chiesi Farmaceutici S.p.A.Inventor: Chiesi Farmaceutici S.p.A.
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Patent number: 8497271Abstract: The present disclosure is generally directed to compounds which can modulate G-protein coupled receptor 88, compositions comprising such compounds, and methods for modulating G-protein coupled receptor 88.Type: GrantFiled: October 1, 2010Date of Patent: July 30, 2013Assignees: Bristol-Myers Squibb Company, Lexicon Pharmaceuticals, Inc.Inventors: Yingzhi Bi, Carolyn Diane Dzierba, Joanne J. Bronson, Kenneth Carson, Giovanni Cianchetta, Li Dong, Cynthia Fink, Michael Green, David Kimball, John E. Macor, Soojin Kwon, Jiancheng Wang, Yulian Zhang, Greg Zipp
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Publication number: 20130190514Abstract: The method of treating patients by administering N-[3-[5-[(4-fluorophenyl)methyl]-2-thienyl]-1-methyl-2-propynyl]-N-hydroxyurea for treatment of leukotriene related pathologies, and compositions for this use.Type: ApplicationFiled: July 25, 2011Publication date: July 25, 2013Applicant: TALLIKUT PHARMACEUTICALS, INC.Inventors: Rebecca Taub, Tilmann Brotz, John Franc, Larry Cohen, Hemantkumar H. Patel, Sanjay R. Chemburkar, David P. Sawick
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Patent number: 8492437Abstract: Compounds of formula (I): in which R1, R2, R7, R8, R9, R10 and A have the meanings given in the specification, are DP2 receptor modulators useful in the treatment of immunologic diseases.Type: GrantFiled: April 17, 2012Date of Patent: July 23, 2013Assignee: Array BioPharma Inc.Inventors: George A. Doherty, Adam Cook
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Publication number: 20130184222Abstract: Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1 comprising administering to a subject in need thereof a compound described here.Type: ApplicationFiled: July 15, 2011Publication date: July 18, 2013Applicant: AGIOS PHARMACEUTICALS, INCInventors: Janeta Popovici-Muller, Francesco G. Salituro, Jeffrey Saunders, Jeremy Travins, Shunqi Yan
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Publication number: 20130183252Abstract: The present invention relates to the discovery that specific human taste receptors in the T2R taste receptor family respond to particular bitter compounds present in, e.g., coffee. Also, the invention relates to the discovery of specific compounds and compositions containing that function as bitter taste blockers and the use thereof as bitter taste blockers or flavor modulators in, e.g., coffee and coffee flavored foods, beverages and medicaments. Also, the present invention relates to the discovery of a compound that antagonizes numerous different human T2Rs and the use thereof in assays and as a bitter taste blocker in compositions for ingestion by humans and animals.Type: ApplicationFiled: February 10, 2012Publication date: July 18, 2013Applicant: Senomyx, Inc.Inventors: Xiaodong LI, Andrew Patron, Catherine Tachdjian, Hong Xu, Qing Li, Alexey Pronin, Guy Servant, Lan Zhang, Thomas Brady, Vincent Darmohusodo, Melissa Arellano, Victor Selchau, Brett Weylan Ching, Donald S. Karanewsky, Paul Brust, Jing Ling, Wen Zhao, Chad Priest
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Patent number: 8487109Abstract: The present invention relates to a process for the regioselective synthesis of compounds of the formula (I), wherein R1; R2; R3; R4; R5; J and W have the meanings indicated in the claims. The present invention provides an efficient and general palladium-catalyzed coupling process for aryl tosylates with terminal alkynes to a wide variety of substituted, multifunctional aryl-1-alkynes of the formula I.Type: GrantFiled: December 23, 2009Date of Patent: July 16, 2013Assignee: SanofiInventors: Omar Rkyek, Marc Nazare, Andreas Lindenschmidt, Matthias Urmann, Nis Halland, Jorge Alonso
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Publication number: 20130157857Abstract: The present invention relates to an inhibitor for tobacco axillary bud growth, the inhibitor comprising, as an active ingredient, one or more kinds of very-long chain fatty acid synthesis inhibitors such as a chloroacetamide-based herbicide, fentrazamide, cafenstrole or indanofan; an inhibitor for tobacco axillary bud growth, the inhibitor comprising the aforesaid very-long chain fatty acid synthesis inhibitor together with clorthal-dimethyl or an aliphatic alcohol having 6 to 20 carbon atoms; and a method for inhibiting tobacco axillary bud growth which comprises applying the inhibitor for tobacco axillary bud growth. The inhibitor for tobacco axillary bud growth of the present invention shows sustained drug efficacy at a low concentration, induces neither chemical injury nor disease, and can contribute to the improvement in labor productivity.Type: ApplicationFiled: July 26, 2011Publication date: June 20, 2013Applicant: SDS BIOTECH K.K.Inventors: Motoki Tanaka, Keijitsu Tanaka, Takeshi Shibuya, Eiji Ikuta, Kotaro Yoshinaga, Yuki Yamaguchi