Having -c(=x)-, Wherein X Is Chalcogen, Attached Indirectly To The Hetero Ring By Nonionic Bonding Patents (Class 549/496)
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Patent number: 11787775Abstract: The invention relates to compounds and methods of using said compounds, as well as pharmaceutical compositions containing such compounds, for treating diseases and conditions mediated by TEAD, such as cancer.Type: GrantFiled: July 22, 2021Date of Patent: October 17, 2023Assignee: Genentech, Inc.Inventors: Jason R. Zbieg, Paul Powell Beroza
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Patent number: 9714215Abstract: A method for producing an isocyanate, comprising: a carbamation step of generating an N-substituted carbamate from an organic primary amine, urea and an organic hydroxy compound according to a carbamation reaction, and then recovering a first gaseous phase component containing the urea and/or a compound having a carbonyl group derived from the urea, the organic hydroxy compound, and ammonia; a condensation step of condensing the first gaseous phase component with a condenser; an isocyanate production step of producing an isocyanate by subjecting the N-substituted carbamate to pyrolysis; an ammonia absorption step of allowing a second gaseous phase component containing ammonia recovered as a gaseous phase component from the condenser as a main component, to be absorbed by absorption water, and generating gas-absorbed water; and an ammonia stripping step of heating the gas-absorbed water to separate ammonia from the gas-absorbed water.Type: GrantFiled: March 28, 2014Date of Patent: July 25, 2017Assignee: Asahi Kasei Chemicals CorporationInventors: Masaaki Shinohata, Kouji Takeuchi, Naoki Fujimoto, Nobuhisa Miyake
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Patent number: 9605112Abstract: The present invention relates to new classes of monomeric compounds, which may be polymerized to form novel biodegradable and bioresorble polymers and copolymers. These polymers and co-polymers, while not limited thereto, may be adapted for radio-opacity and are useful for medical device applications and controlled release therapeutic formulations.Type: GrantFiled: October 11, 2010Date of Patent: March 28, 2017Assignee: RUTGERS, THE STATE UNIVERSITY OF NEW JERSEYInventors: Joachim B. Kohn, Durgadas Bolikal
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Patent number: 9487537Abstract: Dicarbamates of the reduction products of 2-hydroxymethyl-5-furfural (HMF) and a method of preparing the same are described. The method involves reacting a mixture of an isohexide and a cynate salt in a non-aqueous solvent, with a miscible acid having a pKa of about 3.7 or less. The dicarbamates of HMF-reduction products can serve as precursor materials from which various derivative compounds can be synthesized.Type: GrantFiled: May 7, 2014Date of Patent: November 8, 2016Assignee: Archer Daniels Midland Co.Inventor: Kenneth Stensrud
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Patent number: 9447063Abstract: The present invention relates to a novel disubstituted adamantyl derivative or the pharmaceutically acceptable salts thereof, a method for preparing the same, and a pharmaceutical anticancer or antimetastasis composition comprising the same as an active ingredient. The disubstituted adamantyl derivative of the present invention suppressed accumulation of HIF-1?, inhibiting the expression of the metastasis related protein Twist dose-dependently. Thus, the disubstituted adamantyl derivative of the invention is effective in inhibiting the expressions of the metastasis related proteins, ?-catenin and RohA, and the EMT related genes such as MMP2 and MMP9, without cytotoxicity. Therefore, the disubstituted adamantyl derivative or the pharmaceutically acceptable salts thereof of the invention can be efficiently used as a pharmaceutical anticancer or antimetastasis composition.Type: GrantFiled: May 28, 2015Date of Patent: September 20, 2016Assignees: KOREA RESEARCH INSTITUTE OF BIOSCIENCE AND BIOTECHNOLOGY, DONGGUK UNIVERSITY INDUSTRY-ACADEMIC COOPERATION FOUNDATIONInventors: Mi Sun Won, Kyeong Lee, Bo Kyung Kim, Hyun Seung Ban, Seohyun Son, Kyung-Sook Chung
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Publication number: 20150133442Abstract: The invention features compositions and methods for inhibiting the Pin1 protein, and the treatment of disorders characterized by elevated Pin1 levels.Type: ApplicationFiled: June 7, 2013Publication date: May 14, 2015Inventors: Kun Ping Lu, Matthew Brian Boxer, Mindy Irene Emily Davis, Rajan Pragani, Min Shen, Anton Momtchilov Simeonov, Shuo Wei, Xiao Zhen Zhou
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Patent number: 8951999Abstract: This invention relates to compounds of formula I, their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions such as inflammatory/nociceptive pain. A, M, R1, R2, R7, Ra, Rb, Q3, Q4, Q6, Z2, Z4, Z5, Z6 and W have meanings given in the description.Type: GrantFiled: October 20, 2010Date of Patent: February 10, 2015Assignee: Orexo ABInventors: Henning Priepke, Henri Doods, Raimund Kuelzer, Roland Pfau, Dirk Stenkamp, Robert Roenn, Benjamin Pelcman
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Publication number: 20150038466Abstract: The present invention relates to the use of compounds for the treatment or prevention of pain in mammals, in particularly in human beings, and also to a process for preparing these compounds.Type: ApplicationFiled: December 31, 2012Publication date: February 5, 2015Inventors: Sylvie Ducki, Khalil Bennis, Alain Eschalier, Jérôme Busserolles, Florian Lesage, Nuno Rodriguez, Delphine Vivier
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Publication number: 20150011550Abstract: Use of a synthetic compound selected from the group consisting of JKF-006, JKF-011 and JKF-027 in the preparation of a medicament for treating Alzheimer's disease.Type: ApplicationFiled: January 25, 2013Publication date: January 8, 2015Applicant: BEIJING JOEKAI BIOTECHNOLOGY LLCInventor: Weiwei Ma
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Publication number: 20140377219Abstract: Chemical compounds that inhibit retroviruses are presented herein. More particularly, this disclosure provides small molecule compounds that inhibit infection with, or treat infection caused by, human immunodeficiency viruses.Type: ApplicationFiled: September 6, 2012Publication date: December 25, 2014Applicant: New York Blood CEnter, Inc.Inventors: Asim Kumar Debnath, Francesca Curreli, Peter D. Kwong, Young Do Kwon
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Publication number: 20140357682Abstract: Non ligand binding pocket antagonists for the human androgen receptor. The androgen receptor (AR) is a member of the Nuclear Receptor (NR) family and its role is to modulate the biological effects of the endogenous androgens, testosterone (tes) and dihydrotestosterone (DHT). Synthetic androgens and anti-androgens have therapeutic value in the treatment of various androgen dependent conditions, from regulation of male fertility to prostate cancer. Current treatment of prostate cancer (PCa) typically involves administration of ‘classical’ antiandrogens, competitive inhibitors of natural AR ligands, DHT and tes, for the ligand binding pocket (LBP) in the C-terminal ligand binding domain (LBD) of the AR. However, prolonged LBP-targeting can often lead to androgen resistance and alternative therapies and therapeutic strategies are urgently required. Disclosed herein are a class of non-steroidal, small molecule AR antagonists which inhibit the transcriptional activity of the AR by non LBP-mediated modulation.Type: ApplicationFiled: November 23, 2012Publication date: December 4, 2014Applicant: THE PROVOST, FELLOWS, FOUNDATION SCHOLARS, & THE OTHER MEMBERS OF BOARD, OF THE COLLEGE OF THE HOLYInventors: David George Lloyd, Darren Fayne, Mary Jane Meegan, Miriam Carr, Gemma Karena Kinsella, Laura Caboni, Wiliam Nicholas Jagoe, Billy Egan, Fernando Blanco
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Patent number: 8895587Abstract: The present invention provides compounds of formula (I) wherein R1, R2, R3, R4, G1, n, A1, A2, A3, A4, Y1, Y2, and Y3 are as defined in the claims. The invention also relates to processes and intermediates for preparing these compounds, to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising these compounds and to methods of using these compounds to control insect, acarine, nematode and mollusc pests.Type: GrantFiled: May 15, 2012Date of Patent: November 25, 2014Assignee: Syngenta Participations AGInventors: Jerome Yves Cassayre, Myriem El Qacemi, Torsten Luksch, Peter Renold
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Publication number: 20140343049Abstract: The present invention relates to compounds of formula (IA) wherein QA is QA1 or QA2 P is P1, heterocycyl or heterocyclyl substituted by one to five Z; and wherein A1, A2, A3, A4, G1, Z, R1, R2, R3 and R4 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (IA), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising the compounds of formula (IA) and to methods of using the compounds of formula (IA) to control insect, acarine, nematode and mollusc pests.Type: ApplicationFiled: August 10, 2012Publication date: November 20, 2014Applicant: SYNGENTA PARTICIPATIONS AGInventors: Julie Clementine Toueg, Tomas Smejkal, Sebastian Volker Wendeborn, Jerome Yves Cassayre, Myriem El Qacemi, Bernhard Breit, Lisa Diab, Regis Jean Georges Mondiere, Nicolas Poirier
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Publication number: 20140343108Abstract: The present invention belongs to the field of natural medicine and pharmaceutical chemistry, and specifically relates to novel amidated derivatives of oleanolic acid according to formula (I) or a pharmaceutically acceptable salt thereof, to a process for the preparation of these compounds, compositions containing such compounds and their use in preparing antineoplastic medicaments.Type: ApplicationFiled: November 30, 2012Publication date: November 20, 2014Inventors: Frank Rong, Rongzhen Xu, Fuwen Xie, Hongxi Lai
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Publication number: 20140336185Abstract: Compounds that bind the glucagon-like peptide 1 (GLP-1) receptor, methods of their synthesis, methods of their therapeutic and/or prophylactic use, and methods of their use in stabilizing GLP-1 receptor in vitro for crystallization of the GLP-1 receptor are provided. Certain compounds may have activity as modulators or potentiators with respect to glucagon receptor, GIP receptor, GLP-1 and GLP-2 receptors, and PTH receptor on their own or in the presence of receptor ligands such as GIP (1-42), PTH (1-34), Glucagon (1-29), GLP-2 (1-33), GLP-1 (7-36), GLP-1 (9-36), oxyntomodulin and exendin variants.Type: ApplicationFiled: May 31, 2012Publication date: November 13, 2014Inventors: Marcus F. Boehm, Esther Martinborough, Manisha Moorjani, Junko Tamiya, Liming Huang, Thomas Fowler, Andrew Novak, Premji Meghani, Enugurthi Brahmachary, Adam Richard Yeager
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Patent number: 8877754Abstract: The invention relates to new compounds of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.Type: GrantFiled: August 17, 2011Date of Patent: November 4, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Gerald Juergen Roth, Martin Fleck, Heike Neubauer, Bernd Nosse
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Publication number: 20140323518Abstract: Compounds of formula (I) or a pharmaceutically acceptable ester, amide, carbamate or salt thereof, including a salt of such an ester, amide or carbamate in which R1 to R9 have meanings as defined in the Specification, are useful as estrogen receptor ligands.Type: ApplicationFiled: August 2, 2012Publication date: October 30, 2014Inventors: Aiping Cheng, Neeraj Garg, Lars Krüger, Joakim Löfstedt, Eva Koch, Konrad Koehler, Lars Hagberg, Daniel Nöteberg
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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: 20140309426Abstract: The present invention features pharmaceutical compositions and methods of using pharmaceutical compositions for treating left ventricular diastolic dysfunction. In particular, the pharmaceutical compositions include an apolipoprotein complex comprising a lipid fraction and a protein fraction.Type: ApplicationFiled: June 23, 2014Publication date: October 16, 2014Inventors: Jean-Claude TARDIF, David Busseuil, Eric Rhéaume
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Patent number: 8853281Abstract: Compounds of the formula I wherein R1a is H; and R1b is C1-C6 alkyl, Carbocyclyl or Het; or R1a and R1b together define a saturated cyclic amine with 3-6 ring atoms; R2a and R2b are H, halo, C1-C4alkyl, C1-C4haloalkyl, C1-C4alkoxy; or R2a and R2b together with the carbon atom to which they are attached form a C3-C6cycloalkyl; R3 is a branched C5-C10alkyl chain, C2-C4haloalkyl or C3-C7cycloalkylmethyl, R4 is Het, Carbocyclyl, optionally substituted as defined in the specification and pharmaceutically acceptable salts, hydrates and N-oxides thereof; are inhibitors of cathepsin S and have utility in the treatment of psoriasis, autoimmune disorders and other disorders such as asthma, arteriosclerosis, COPD and chronic pain.Type: GrantFiled: December 18, 2009Date of Patent: October 7, 2014Assignee: Medivir UK LtdInventors: Susana Ayesa, Anna Karin Belfrage, Bjorn Classon, Urszula Grabowska, Ellen Hewitt, Vladimir Ivanov, Daniel Jönsson, Pia Kahnberg, Peter Lind, Magnus Nilsson, Lourdes Odén, Mikael Pelcman, Horst Wähling
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Publication number: 20140275112Abstract: Disclosed herein are methods and compositions comprising compounds capable of normalizing neuronal calcium dyshomeostasis. Also disclosed are methods comprising these compounds for treating neuronal or neurological disorders, including Alzheimer's disease, Parkinson's disease, Huntington's disease, fronto-temporal dementia, Pick's disease, chronic traumatic encepholopathy, traumatic brain injury, stroke, cerebellar ataxia, multiple sclerosis, Down syndrome, and aging-related CNS disorders.Type: ApplicationFiled: March 14, 2014Publication date: September 18, 2014Applicant: Rosalind Franklin University of Medicine and ScienceInventors: Grace E. Stutzmann, Russell Dahl
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Publication number: 20140235533Abstract: The present invention provides compounds of formula I wherein Q is Q1 or Q2; A1, A2, A3 and A4 are independently of each other C—H, C—R7, or nitrogen; R1 is C1-C8haloalkyl; R2 is aryl or aryl substituted by one to five R11, or heteroaryl or heteroaryl substituted by one to five R11; and R3, R4, R5, R6 and R7 are as defined in the claims. The invention also provides methods of controlling insects, acarines, nematodes or molluscs which methods comprise applying to a pest, to a locus of a pest, or to a plant susceptible to attack by a pest an insecticidally, acaricidally, nematicidally or molluscicidally effective amount of a compound of formula (I).Type: ApplicationFiled: August 10, 2012Publication date: August 21, 2014Applicant: SYNGENTA PARTICIPATIONS AGInventors: Tomas Smejkai, Sebastian Volker Wendeborn, Jerome Yves Cassayre, Myriem El Qacemi, Bernhard Breit, Lisa Diab, Regis Jean Georges Mondiere
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Publication number: 20140206651Abstract: The invention relates to a compound of formula (I): or a pharmaceutically acceptable salt thereof, thereof, wherein: G is a group of formula (II): and pharmaceutically acceptable salts, prodrugs, hydrates, or solvates, thereof, wherein A, B, L1-L4, A, B, R1-R4, and m are as defined herein. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and their use in treating a bacterial infection.Type: ApplicationFiled: March 24, 2014Publication date: July 24, 2014Applicant: Pfizer Inc.Inventors: Matthew Frank Brown, Charles Francis Donovan, Edmund Lee Ellsworth, Denton Wade Hoyer, Timothy Allan Johnson, Manjinder Singh Lall, Chris Limberakis, Sean Timothy Murphy, Debra Ann Sherry, Clarke Bentley Taylor, Joseph Scott Warmus
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Patent number: 8785451Abstract: Disclosed are compounds of formula (IA), formula (IV) or formula (V), wherein the variables are as defined herein, and pharmaceutical compositions containing them which are useful for treating a subject with a proliferative disorder, such as cancer. The disclosed compounds and pharmaceutical compositions are also useful for treating disorders responsive to Hsp70 induction and/or natural killer induction.Type: GrantFiled: August 20, 2007Date of Patent: July 22, 2014Assignee: Synta Pharmaceuticals Corp.Inventors: Keizo Koya, Lijun Sun, Shoujun Chen, Jun Jiang
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Patent number: 8722686Abstract: The invention relates to a compound of formula (I): or a pharmaceutically acceptable salt thereof, thereof, wherein: G is a group of formula (II); and pharmaceutically acceptable salts, prodrugs, hydrates, or solvates, thereof, wherein A, B. L1-L4 A, B, R1-R4 and m are as defined herein. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and their use in treating a bacterial infection.Type: GrantFiled: September 1, 2009Date of Patent: May 13, 2014Assignee: Pfizer Inc.Inventors: Matthew F. Brown, Charles F. Donovan, Edmund L. Ellsworth, Denton W. Hoyer, Timothy A. Johnson, Manjinder S. Lall, Chris Lim-Berakis, Sean T. Murphy, Debra A. Sherry, Clarke B. Taylor, Joseph S. Warmus
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Publication number: 20140116293Abstract: The present invention relates to a cellulose acetate film for optical compensation and a retardation enhancer used therein, and relates to a cellulose acetate film which has a high retardation value in the thickness direction (Rth).Type: ApplicationFiled: June 20, 2012Publication date: May 1, 2014Applicant: SK INNOVATION CO., LTD.Inventors: Won Yeob Kim, Min Joung Im, Seung Eon Lee, Hyo Shin Kwak, Myoung Lae Kim, Yong Gyun Cho
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Publication number: 20140112892Abstract: The purpose is to select low-molecular-weight compounds which are effective in inducing differentiation of mesenchymal stem cell into hepatocyte and to develop a safe differentiation-inducing method having excellent efficiency of differentiating mesenchymal stem cell into hepatocyte. Provided are at least one compound selected from the group consisting of compounds represented by formulae (1) and (2), a salt thereof, or a solvate of them; a differentiation inducer comprising at least one compound selected from the group consisting of compounds represented by formulae (1) and (2), a salt thereof, or a solvate of them; and a differentiation inducer comprising a compound represented by formula (8), a salt thereof, or a solvate of them.Type: ApplicationFiled: April 2, 2012Publication date: April 24, 2014Applicants: NATIONAL UNIVERSITY CORPORATION TOTTORI UNIVERSITY, TOKYO WOMEN'S MEDICAL UNIVERSITY, NATIONAL UNIVERSITY CORPORATION TOTTORI UNIVERSITY, TOKYO WOMEN'S MEDICAL UNIVERSITYInventors: Goshi Shiota, Yoshiko Hoshikawa, Noriko Matsumoto, Yoshiaki Matsumi, Minoru Morimoto, Takayuki Tonoi, Hiroyuki Saimoto, Kazuo Ohashi, Teruo Okano
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Publication number: 20140107161Abstract: The present invention provides compounds of formula (I) wherein R1, R2, R2, R3, R4, G1, n, A1, A2, A3, A4, Y1, Y2, and Y3 are as defined in the claims. The invention also relates to processes and intermediates for preparing these compounds, to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising these compounds and to methods of using these compounds to control insect, acarine, nematode and mollusc pests.Type: ApplicationFiled: May 12, 2012Publication date: April 17, 2014Applicant: SYNGENTA PARTICIPATIONS AGInventors: Jerome Yves Cassayre, Myriem El Qacemi, Torsten Luksch, Peter Renold
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Publication number: 20130308219Abstract: The present invention relates to a polymerizable composition comprising at least one ethylenically unsaturated, polymerizable compound and at least one oxime sulfonate compound of the formula (I) QAaBbCc where a is 0, 1, 2, 3, 4 or 6, b is 0, 1, 2, 3, 4 or 6, and c is 0, 1, 2, 3, 4 or 6, where the sum of a+b+c is 1, 2, 3, 4 or 6 where (A) is a group (B) is a group (C) is a group where # denotes the point of attachment to Q; X is S or NR14 and Q, R1, R2, R3 and R14 are as defined in claim 1 and in the description. The present invention also relates to the use of the this composition, to novel oxime sulfonates and the use of the oxime sulfonates as thermal curing promoter.Type: ApplicationFiled: January 27, 2012Publication date: November 21, 2013Applicant: BASF SEInventors: Kazuhiko Kunimoto, Kaori Sameshima, Yuki Matsuoka, Hisatoshi Kura
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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: 20130245275Abstract: The present invention relates to phenyl diamides according to the general formula (1) and their use as a medicament and a pharmaceutical preparation comprising as an active ingredient a phenyl diamide according to the general formula (1). Further, the present invention relates to phenyl diamides according to the formulas (16), (17) and (18) for use in the treatment of gliomas.Type: ApplicationFiled: October 4, 2011Publication date: September 19, 2013Applicant: Rheinische Friedrich-Wilhelms Universitaet BonnInventors: Michael Famulok, Anke Bill, Anton Schmitz, Juergen Bajorath
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Publication number: 20130237711Abstract: Intermediates and methods of their use in the synthesis of analogs of halichondrin B are provided.Type: ApplicationFiled: April 23, 2013Publication date: September 12, 2013Applicant: Eisai R&D Management Co., Ltd.Inventors: Farid BENAYOUD, Trevor Lee Calkins, Charles E. Chase, William Christ, Francis G. Fang
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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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Patent number: 8466301Abstract: An organic dye used in a dye-sensitized solar cell is described, having general formula (1): wherein Ar1 represents a substituted or unsubstituted arylene group, Ar2 and Ar3 each independently represent a substituted or unsubstituted aryl group, Sp1 represent a single bond or a spacer group allowing conjugation between Ar1 and the furan moiety, Sp2 represent a single bond or a spacer group allowing conjugation between the furan moiety and Ac, Ac represents an acceptor group, and Y represents an anchoring group.Type: GrantFiled: July 24, 2009Date of Patent: June 18, 2013Assignees: Academia Sinica, Plasmag Technology Inc.Inventors: Jiann Tsuen Lin, Yung-Sheng Yen, Ying-Chan Hsu, Ming-Chang Yeh, Pin-Cheng Chen
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Publication number: 20130131340Abstract: Estrogen-Related Receptor (ERR) modulating compounds and methods for synthesis of said compounds are described.Type: ApplicationFiled: September 20, 2011Publication date: May 23, 2013Inventors: Barry Forman, Donna Yu
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Publication number: 20130129646Abstract: The present invention relates to the cosmetic, dermatological or pharmaceutical (therapeutic) use of compounds of formula (I) or a cosmetically acceptable salt of a compound of formula (I) or a mixture containing two or more of these compounds or the salts thereof wherein R1 denotes hydrogen or an organic radical having 1 to 14 carbon atoms, R2 denotes an organic radical having 1 to 14 carbon atoms, and wherein optionally R1 and R2 are covalently bonded to one another, preferably so that a 3 to 8 membered ring is formed, for the lightening of skin and/or hair. The invention further relates to compositions and cosmetic, dermatological or pharmaceutical preparations (compositions) comprising one or more compounds of formula (I) suitable for lightening human skin and/or hair and corresponding methods.Type: ApplicationFiled: May 25, 2010Publication date: May 23, 2013Inventors: Gabriele Vielhaber, Heiko Oertling, Karin Schaper, Claudia Gömann, Rahim Brodhage
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Publication number: 20130109750Abstract: The invention relates to novel arylamide derivatives having formula (I) and stereoisomers and pharmaceutically acceptable salts thereof, where R1-R11, R?, R?, z and X are as defined in the claims. The arylamide derivatives of formula (I) have antiandrogenic properties. The invention also relates to compounds of formula (I) for use as a medicament and to pharmaceutical compositions comprising them and to their preparation.Type: ApplicationFiled: July 14, 2011Publication date: May 2, 2013Applicant: MEDEIA THERAPEUTICS LTDInventors: Jari Ratilainen, Milla Koistinaho, Anu Muona
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Publication number: 20130096129Abstract: The present invention provides compounds of Formulae (A), (B), (C), and (D), pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, and prodrugs thereof, pharmaceutical compositions thereof, and kits thereof. The present invention further provides methods of using the compounds to treat or prevent neurological disorders. In one aspect, the methods include administering to a subject in need of treatment for a neurological disorder a therapeutically effective amount of DAC-001, DAC-002, DAC-003, DAC-009, or DAC-012, or a compound of Formula (A), (B), (C), or (D).Type: ApplicationFiled: July 20, 2012Publication date: April 18, 2013Inventors: Li-Huei Tsai, Ling Pan, Stephen J. Haggarty, Debasis Patnaik
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Publication number: 20130096092Abstract: Disclosed are inhibitors of retroviral growth of formula (I), that are useful in treatment of retroviral infections such as HIV. Also disclosed are a composition comprising a pharmaceutically acceptable carrier and at least one compound or salt of the invention, a method for inactivating a virus, a method for dissociating a metal ion from a zinc finger-containing protein, and a method for inhibiting the transmission of a virus.Type: ApplicationFiled: June 10, 2011Publication date: April 18, 2013Applicants: Health and Human ServicesInventors: Daniel Appella, Ettore Appella, John K. Inman, Lisa M. Miller Jenkins, Ryo Hayashi, Deyun Wang
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Publication number: 20130096175Abstract: Provided are compounds which generally have a triketone structure. Examples of the compounds include derivatives of 1,3-cyclohexanedione, such as: 1,3-cyclohexanedione, 2-propanoyl-5-cyclohexyl-; 1,3-cyclohexanedione, 2-propanoyl-5-[4-fluorophenyl]-; 1,3-cyclohexanedione, 2-acetyl-5-[thien-2-yl]-; 1,3-cyclohexanedione, 2-acetyl-5-butyl-; and 1,3-cyclohexanedione, 2-propanoyl-5-[bicyclo[2.2.1]hept-2-en-5-yl]-. The compounds can be used to alter the lifespan of eukaryotic organisms and treat inflammation.Type: ApplicationFiled: November 17, 2010Publication date: April 18, 2013Applicants: SOUTHERN RESEARCH INSTITUTE, UNIVERSITY OF ROCHESTERInventors: David S. Goldfarb, Joseph A. Maddry, Lynn Rasmussen, Ellie Lucile White, Krister Wennerberg
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Publication number: 20130072520Abstract: Compounds of formula (I) have antibacterial activity: wherein R represents hydrogen or 1, 2 or 3 optional substituents; W is ?C(R1)— or ?N—; R1 is hydrogen or an optional substituent 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—; R3 is a radical of formula -(Alk1)m-(Z)p-(Alk2)n-Q wherein m, p and n are independently 0 or 1, provided that at least one of m, p and n is 1, Z is —O—, —S—, —S(O)—, —S(O2)—, —NH—, —N(CH3)—, —N(CH2CH3)—, —C(?O)—, —O—(C?O)—, —C(?O)—O—, or an optionally substituted divalent monocyclic carbocyclic or heterocyclic radical having 3 to 6 ring atoms; or an optionally substituted divalent bicyclic heterocyclic radical having 5 to 10 ring atoms; Alk1 and Alk2 are optionally substituted C1-C6 alkylene, C2-C6 alkenylene, or C2-C6 alkynylene radicals, which may optionally terminate with or be interrupted by —O—, —S—, —S(O)—, —S(O2)—, —NH—, —N(CH3)—, or —N(CH2CH3)—; and Q is hydrogen, halogen, nitType: ApplicationFiled: November 28, 2011Publication date: March 21, 2013Applicant: Biota Scientific Management Pty LtdInventors: David BROWN, Ian COLLINS, Lloyd CZAPLEWSKI, David HAYDON
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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: 20130035328Abstract: The invention relates to compounds having antiviral activity and methods utilizing the compounds to treat viral infections.Type: ApplicationFiled: July 19, 2012Publication date: February 7, 2013Inventors: Peter William Gage, Gary Dinneen Ewart, Lauren Elizabeth Wilson, Wayne Best, Anita Premkumar
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ACYLAMINO-SUBSTITUTED FUSED CYCLOPENTANECARBOXYLIC ACID DERIVATIVES AND THEIR USE AS PHARMACEUTICALS
Publication number: 20130030008Abstract: The present invention relates to compounds of the formula I, wherein A, Y, Z, R3 to R6, R20 to R22 and R50 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.Type: ApplicationFiled: October 1, 2012Publication date: January 31, 2013Applicant: SANOFIInventor: Sanofi -
Publication number: 20120329769Abstract: The present invention relates to compounds of formula (I) wherein Q is Q1 or Q2 P is P1, heterocyclylor heterocyclyl substituted by one to five Z; and wherein A1, A2, A3, A4, G1, Y1, Z, R1, R2, R3 and R4 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising the compounds of formula (I) and to methods of using the compounds of formula (I) to control insect, acarine, nematode and mollusc pests.Type: ApplicationFiled: January 31, 2011Publication date: December 27, 2012Applicant: SYNGENTA CROP PROTECTION LLCInventors: Myriem El Qacemi, Jerome Yves Cassayre, Julie Clementine Toueg, Peter Renold, Thomas Pitterna
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Publication number: 20120214782Abstract: The invention relates to new compounds of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.Type: ApplicationFiled: August 17, 2011Publication date: August 23, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Gerald Juergen ROTH, Martin FLECK, Heike NEUBAUER, Bernd NOSSE
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Publication number: 20120121527Abstract: 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: January 18, 2012Publication date: May 17, 2012Applicant: Galderma Research & DevelopmentInventors: Jean-Guy BOITEAU, Laurence Clary, Corinne Millois Barbuis
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Publication number: 20120122918Abstract: Compounds of formula (1) 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)-Q.Type: ApplicationFiled: November 28, 2011Publication date: May 17, 2012Applicant: BIOTA SCIENTIFIC MANAGEMENT PTY LTDInventors: David Ryall BROWN, Ian COLLINS, Lloyd George CZAPLEWSKI, David John HAYDON
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Publication number: 20120115851Abstract: An objective of the present invention is to provide compounds that can effectively suppress the concentration of phosphorus in serum to effectively prevent or treat diseases induced by an increase in concentration of phosphate in serum. The compounds according to the present invention are compounds represented by formula (I) and pharmaceutically acceptable salts and solvates thereof: wherein A represents an optionally substituted five- to nine-membered unsaturated carbocyclic moiety or a five- to nine-membered unsaturated heterocyclic moiety, and represents a single bond or a double bond, R5 represents optionally substituted aryl or the like, Z represents —N?CHR6R7 or the like, R6 and R7 represent H, optionally substituted alkyl, optionally substituted aryl or the like, R101 and R102 together form ?O, and R103 and R104 represent H, or R101 and R104 together from a bond, and R102 and R103 together form a bond.Type: ApplicationFiled: January 18, 2012Publication date: May 10, 2012Applicant: KYOWA HAKKO KIRIN CO., LTD.Inventors: Nobuaki Eto, Rika Nagao, Tetsuko Kazama
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Patent number: 8173700Abstract: The present invention relates to salts of substituted allophanates, methods for their production, medicaments containing said compounds and the use of said compound for the production of medicaments.Type: GrantFiled: May 17, 2006Date of Patent: May 8, 2012Assignee: Gruenenthal GmbHInventors: Robert Frank, Ruth Jostock, Hans Schick, Fritz Theil, Olga Groeger, Rene Kudick, Helmut Sonnenschein, Birgitta Henkel