Acyclic Chalcogen Bonded Directly To The Hetero Ring Patents (Class 549/395)
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Publication number: 20150057166Abstract: Certain embodiments provide a method for crystallizing a GPCR. The method may employ a fusion protein comprising, from N-terminus to C-terminus: a) a first portion of a family C G-protein coupled receptor (GPCR), wherein the first portion comprises the TM1, TM2 and TM3, regions of the GPCR; b) a stable, folded protein insertion; and c) a second portion of the GPCR, wherein the second portion comprises the TM4, TM5 TM6 and TM7 regions of the GPCR.Type: ApplicationFiled: October 17, 2014Publication date: February 26, 2015Inventor: BRIAN KOBILKA
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Publication number: 20120321714Abstract: The present invention relates to a solid pharmaceutical composition including the active principle 6-oxo-6,7,8,9,10,11-hexahydrocyclohepta[c]chromen-3-yl sulfamate. The present invention also relates to polymorphs of the 6-oxo-6,7,8,9,10,11-hexahydrocyclohepta[c]chromen-3-yl sulfamate compound.Type: ApplicationFiled: March 26, 2012Publication date: December 20, 2012Applicant: Ipsen Pharma S.A.S.Inventors: Nathalie MONDOLY, Bertrand Poirot, Anne Brochard, Joël Richard, Delphine Delahaye, Christian Diolez, Alain Rolland, Francis Diancourt, Gérard Coquerel, Damien Martins, Julie Linol, Marie-Noêlle Petit, Barry Victor Llyod Potter, Lok, Wai Lawrence Woo
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Patent number: 8039648Abstract: Compounds used as dyes comparable to Alexa Fluor 350 dyes. The inventive compounds have high fluorescence quantum yield and high photostability. The dyes facilitate analysis of biological structures with enhanced sensitivity and selectivity.Type: GrantFiled: June 16, 2009Date of Patent: October 18, 2011Assignee: Pierce Biotechnology, Inc.Inventors: Peter T. Czerney, Surbhi Desai, Matthias S. Wenzel, Boguslawa Dworecki, Frank G. Lehmann, Bernd G. Schweder, Wilhelm G. Frank
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Publication number: 20110020448Abstract: Provided is a pharmaceutical composition for the treatment and prevention of glaucoma, containing (a) a therapeutically effective amount of a compound represented by Formula 1 or a pharmaceutically acceptable salt, prodrug, solvate or isomer thereof, and (b) a pharmaceutically acceptable carrier, diluent or excipient or any combination thereof.Type: ApplicationFiled: December 18, 2008Publication date: January 27, 2011Applicants: MAZENCE, INC., KT & G CORPORATIONInventors: Myung-Gyu Park, Taehwan Kwak
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Patent number: 7019024Abstract: The invention provides a pharmaceutical for treatment of neurological and neuropsychiatric disorders comprising a compound of the formula: or a pharmaceutically acceptable salt thereof.Type: GrantFiled: January 9, 2001Date of Patent: March 28, 2006Assignee: Allelix Neuroscience Inc.Inventors: Vassil Iliya Ognyanov, Laurence A. Borden, Stanley Charles Bell, Jing Zhang
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Publication number: 20030171423Abstract: Resistance-repellent and multidrug resistant retroviral protease inhibitors are provided. Pharmaceutical composition comprising such compounds, and methods of using such compounds to treat HIV infections in mammals, are also provided.Type: ApplicationFiled: January 7, 2003Publication date: September 11, 2003Inventors: John W. Erickson, Michael Eissenstat, Abelardo Silva, Sergei Gulnik
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Patent number: 5763625Abstract: 3-Substituted-.beta.-lapachone analogs and their use either alone or to augment chemotherapy or radiotherapy to induce programmed neoplastic cell death without exhibiting toxicity to surrounding normal cells are disclosed. In particular, 3-allyl-.beta.-lapachones, 3-alkyl-.beta.-lapachones and 3-halo-.beta.-lapachones were found to be Topoisomerase (Topo I) inhibitors. When these analogs are used alone there is a reversible single-strand break in the DNA of neoplastic cells causing apoptosis and cell death in some cells. However, when these analogs are combined with chemotherapy or X-irradiation, an irreversible Topo I-mediated break is achieved. A new and more efficient chemical synthesis of the compounds is also disclosed.Type: GrantFiled: April 25, 1995Date of Patent: June 9, 1998Assignee: Wisconsin Alumni Research FoundationInventors: David A. Boothman, Benjamin J. Frydman, Donald T. Witiak
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Patent number: 5672621Abstract: Carbonarins A, B, C, D, E, F, G, and H have been isolated from the sclerotia of the fungus Aspergillus carbonarius. The carbonarius are effective for controlling Coleopteran and Lepidopteran insects. The carbonarins have the structure: ##STR1## wherein: R.sub.1 is a hydrogen atom or a hydroxy group; R.sub.2 is a hydrogen atom or a methoxy group; R.sub.3 is a hydrogen atom or a naphthopyrone group; and X is an oxygen atom or an NH group.Type: GrantFiled: February 27, 1996Date of Patent: September 30, 1997Assignees: The United States of America as represented by the Secretary of Agriculture, University of Iowa Research Foundation and Biotechnology Research and Development Corp.Inventors: Ali A. Alfatafta, Patrick F. Dowd, James B. Gloer, Donald T. Wicklow
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Patent number: 5300646Abstract: A novel heterocyclic amine derivative of the general formula: ##STR1## wherein a ring A and a ring B stand independently for an optionally substituted benzene ring, Z.sup.o stands for O or S or ##STR2## stands for --CH.sub.2 --, X stands for O, S or NR.sup.1 wherein R.sup.1 stands for hydrogen atom or an alkyl group, Y stands for NH, O or (CH.sub.2).sub.n wherein n denotes 0 to 2, and R.sup.2 stands for an optionally substituted hydrocarbon group, or their salts.Type: GrantFiled: December 22, 1992Date of Patent: April 5, 1994Assignee: Takeda Chemical Industries, Ltd.Inventors: Hideaki Natsugari, Hiroyuki Tawada, Hitoshi Ikeda
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Patent number: 5189183Abstract: Novel aromatic amine derivatives of specific structure are useful intermediates for herbicides. The aromatic amine compounds have the structure shown by formula [I]: ##STR1## wherein Ar and A are as defined herein.Type: GrantFiled: October 16, 1990Date of Patent: February 23, 1993Assignee: Mitsui Petrochemical Industries, Ltd.Inventors: Daisuke Fukuoka, Katsuya Takahashi, Isao Hashimoto
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Patent number: 5137911Abstract: An isochromane derivative having the general formula I ##STR1## in which each of R.sub.1, R.sub.2, and R.sub.3 is one to four substituents independently selected from hydrogen, hydroxy, alkyl (1-4 C), alkoxy (1-4 C), halogen, or CF.sub.3, or represents a methylenedioxy group;R.sub.4 is selected from hydrogen or alkyl (1-4 C);Alk is an alkylene group with 1-4 carbon atoms;Alk' is an alkylene group with 2-4 carbon atoms, when R.sub.5 is selected from hydrogen or alkyl (1-4 C) and X is O or S; orAlk' is an alkylene group with 1-4 carbon atoms or a bond, when R.sub.5 is an alkyl (1-4 C) group and X is CH.sub.2 or a bond;or a pharmaceutically acceptable salt thereof.Type: GrantFiled: April 2, 1991Date of Patent: August 11, 1992Assignee: Akzo N.V.Inventors: Michael Combourieu, Jean-Claude Laigle
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Patent number: 5041565Abstract: Novel hydrazinocarbonyloxylabdanes, intermediates and processes for the preparation thereof, and a method for treating cardiac failure utilizing compounds or compositions thereof are disclosed.Type: GrantFiled: August 30, 1989Date of Patent: August 20, 1991Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Raymond W. Kosley, Jr., Gerard J. O'Malley
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Patent number: 4853410Abstract: Racemic and chiral (2R,4R)-4-c-hydroxy-2-4-(substituted)chroman(and thiochroman)-4-acetic acids and their pharmaceutically acceptable salts, their use in the treatment of diabetic complications and intermediates therefor.Type: GrantFiled: October 9, 1987Date of Patent: August 1, 1989Assignee: Pfizer Inc.Inventor: Christopher A. Lipinski
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Patent number: 4713453Abstract: The present invention relates to a novel oxabicycloheptane derivative of the following formula and a pharmaceutically acceptable salt thereof: ##STR1## where D is a hydrogen atom, a halogen atom, a hydroxyl group, an alkoxy group, an arylalkoxy group, an acyloxy group, a dialkylcarbamoyloxy group or an amidoalkyloxy group; B is a substituted or unsubstituted phenyl, thienyl or furyl group; A is the group ##STR2## (where l is 0 or 1; m and n are each 1 or more, provided that m+n is an interger of 2-8; R.sup.1 is an alkylamino group, a dialkylamino group, an arylalkylamino group, a morpholino group, a thiomorpholino group, a 1-pyrrolidinyl group, a piperidino group, an N-alkylpiperazinyl group, an N-hydroxyalkylpiperazinyl or a pyrrolizidinyl group; and R.sup.2 is a lower alkyl group or a hydroxl group), or the group ##STR3## (where l, m, n, R.sup.1 and R.sup.2 are each the same as defined above), or the group ##STR4## (where R.sup.3 and R.sup.Type: GrantFiled: February 27, 1987Date of Patent: December 15, 1987Assignee: Suntori LimitedInventors: Toshio Tatsuoka, Kenji Suzuki, Kayoko Imao, Fumio Satoh, Seiji Miyano, Kunihiro Sumoto
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Patent number: 4598090Abstract: The present invention relates to new condensed benzopyrone derivatives, to a process for their preparation and to pharmaceutical compositions containing them.Type: GrantFiled: March 22, 1984Date of Patent: July 1, 1986Assignee: Farmitalia Carlo Erba, S.p.A.Inventors: Gianfederico Doria, Carlo Passarotti, Ada Buttinoni