Phosphorus Attached Directly To The Five-membered Hetero Ring By Nonionic Bonding Patents (Class 548/412)
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Patent number: 8828974Abstract: The present invention relates to a series of substituted 3-aminopropane phosphinic acid derivatives of formula I: wherein R, R1, P1, P2 and P3 are as defined herein. The compounds of this invention are useful in treating a variety of diseases including but not limited to depression, anxiety, certain psychiatric symptoms, cognitive impairment and schizophrenia.Type: GrantFiled: April 24, 2012Date of Patent: September 9, 2014Assignee: Aventis Pharmaceuticals Inc.Inventors: Yong Mi Choi-Sledeski, Julian Levell, Gregory Bernard Poli, Mark Czekaj, Alan John Collis, Roy Vaz
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Publication number: 20140199600Abstract: The present invention provides a nonaqueous electrolyte solution, which can improve flame retardancy and ameliorate performances of a battery without deteriorating the basic battery performance as far as possible, and a secondary battery. The nonaqueous electrolyte solution is a nonaqueous electrolyte solution for a secondary battery that contains metal salts including ions of metals belonging to group 1 or 2 of the periodic table and a specific cyclic compound having phosphorus and nitrogen atoms in a non-protonic solvent. The non-protonic solvent is a solvent that contains at least one kind of carboxylic acid ester compound and carbonic acid ester compound, and a ratio (MPN/Ms) between a mass (Ms) of the non-protonic solvent containing the metal salts and a mass (MPN) of the cyclic compound is 0.01 to 1.Type: ApplicationFiled: March 18, 2014Publication date: July 17, 2014Applicant: FUJIFILM CORPORATIONInventors: Toshihiko YAWATA, Ikuo KINOSHITA
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Patent number: 8697902Abstract: A process for the hydrocyanation of a hydrocarbon-based compound having at least one site of ethylenic unsaturation into a nitrile compound includes reaction thereof, in a liquid medium, with hydrogen cyanide in the presence of a catalyst containing a metal element selected from among the transition metals and an organophosphorus ligand, wherein the organophosphorus ligand is a compound of formula (I): The subject process is particularly useful for the synthesis of adiponitrile from butadiene.Type: GrantFiled: June 5, 2009Date of Patent: April 15, 2014Assignee: Rhodia OperationsInventor: Sergio Mastroianni
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Patent number: 8524628Abstract: Provided are a catalyst composition comprising a bidentate ligand, a monodentate ligand, and a transition metal catalyst and a process of hydroformylation of olefin compounds, comprising reacting the olefin compound with a gas mixture of hydrogen and carbon monoxide while being stirred at elevated pressures and temperatures in the presence of the catalyst composition to produce an aldehyde. The catalytic composition demonstrates the high catalytic activity and option control of selectivity to normal aldehyde or iso aldehyde (N/I selectivity) to a desired value.Type: GrantFiled: July 3, 2004Date of Patent: September 3, 2013Assignee: LG Chem, Ltd.Inventors: You Moon Jeon, Dong Hyun Ko, O Hak Kwon, Sung Shik Eom, Sang Gi Lee, Ji Joong Moon, Kwang Ho Park
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Patent number: 8470870Abstract: Solid forms comprising a compound useful in the treatment, prevention and management of various conditions and diseases are provided herein. In particular, provided herein are solid forms comprising (2-carbamoyl-5-chloro-1H-indol-3-yl)-[3-((E)-2-cyano-vinyl)-5-methyl-phenyl]-(R)-phosphinic acid methyl ester, including salts thereof, having utility for the treatment, prevention and management of conditions and disorders including, but not limited to, human immunodeficiency virus infection.Type: GrantFiled: March 27, 2009Date of Patent: June 25, 2013Assignee: Idenix Pharmaceuticals, Inc.Inventors: Adel M. Moussa, Mike H. O'Neill, Xiaohong Sheng
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Publication number: 20130126792Abstract: The present invention relates to compounds of the formula (I), to the use of compounds of the formula (I) in electronic devices and electronic devices comprising one or more compounds of the formula (I). The invention furthermore relates to the preparation of the compounds of the formula (I) and to formulations comprising one or more compounds of the formula (I).Type: ApplicationFiled: July 12, 2011Publication date: May 23, 2013Applicant: Merck Patent GmbHInventors: Irina Martynova, Adam W. Franz, Christof Pflumm, Amir Hossain Parham, Arne Buesing, Rémi Manouk Anémian, Anja Gerhard
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Patent number: 8334317Abstract: The present invention relates generally to novel calcimimetic compounds and pharmaceutical compositions comprising them. The invention also relates to methods of treating of diseases or disorders related to the function of the calcium sensing receptor using the compounds represented in Formula I.Type: GrantFiled: October 15, 2008Date of Patent: December 18, 2012Assignee: Amgen Inc.Inventors: Thomas S. Coulter, Christopher H. Fotsch, Chiara Ghiron, Paul E. Harrington, Michael G. Kelly, Philip Miller, Gilbert M. Rishton, David J. St. Jean, Jr., David J. Semin
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Publication number: 20120197025Abstract: The invention relates to the synthesis of tetraphenol-substituted structures, in particular meta-substituted xylenes. Said tetraphenol-type structures are reacted to obtain organic phosphorus compounds, in particular organophosphites. The invention further relates to the production of catalytically active compositions which contain transition metals in addition to the aforementioned organic phosphorus compounds. According to another subject matter of the invention, said catalytically active compositions are used in chemical reactions with small molecules, e.g. HCN, CO, hydrogen, and amines.Type: ApplicationFiled: August 26, 2010Publication date: August 2, 2012Applicant: Evonik Oxeno GmbHInventors: Andrea Christiansen, Robert Franke, Dirk Fridag, Dieter Hess, Burkard Kreidler, Dieter Vogt, Laura Bini, Michele Janssen, Bart Hamers
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Patent number: 8212056Abstract: The present invention relates to indolyl phosphine ligands, and methods of making such ligands utilizing phenyl hydrazines and aryl ketones as the starting material. The present invention further includes uses of the ligands in the synthesis of pharmaceuticals, materials, and agriculture.Type: GrantFiled: June 30, 2008Date of Patent: July 3, 2012Assignee: The Hong Kong Polytechnic UniversityInventors: Fuk Yee Kwong, Chau Ming So
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Patent number: 8183231Abstract: The present invention relates to a series of substituted 3-aminopropane phosphinic acid derivatives of formula I: wherein R, R1, P1, P2 and P3 are as defined herein. The compounds of this invention are useful in treating a variety of diseases including but not limited to depression, anxiety, certain psychiatric symptoms, cognitive impairment and schizophrenia.Type: GrantFiled: October 24, 2006Date of Patent: May 22, 2012Assignee: Aventis Pharmaceuticals Inc.Inventors: Yong Mi Choi-Sledeski, Julian Levell, Gregory Bernard Poli, Mark Czekaj, Alan John Collis, Roy Vaz
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Patent number: 8110709Abstract: The present invention relates to a process for the hydroformylation of ethylenically unsaturated compounds by reaction with carbon monoxide and hydrogen in the presence of a catalytically active fluid which comprises a dissolved metal complex of a metal of transition group VIII of the Periodic Table of the Elements with at least one phosphoramidite compound as ligand, wherein the fluid is brought into contact with a base.Type: GrantFiled: October 22, 2004Date of Patent: February 7, 2012Assignee: BASF SEInventors: Rainer Papp, Wolfgang Ahlers, Thomas Mackewitz, Rocco Paciello, Martin Volland
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Publication number: 20110070194Abstract: Provided are pyrrolo[1,2-f][1,2,4]triazinyl, imidazo[1,5-f][1,2,4]triazinyl, imidazo[1,2-f][1,2,4]triazinyl, and [1,2,4]triazolo[4,3-f][1,2,4]triazinyl nucleosides, nucleoside phosphates and prodrugs thereof, wherein the 2? position of the nucleoside sugar is substituted with halogen and carbon substitutents. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections caused by both wild type and mutant strains of HCV.Type: ApplicationFiled: September 20, 2010Publication date: March 24, 2011Applicant: Gilead Sciences, Inc.Inventors: Aesop Cho, Choung U. Kim, Samuel E. Metobo, Adrian S. Ray, Jie Xu
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Publication number: 20110057184Abstract: Disclosed is an organic electroluminescent device (organic EL device) that is improved in the luminous efficiency, fully secured of the driving stability, and of a simple structure and disclosed also is a compound useful therefor. The organic EL device comprises a light-emitting layer disposed between an anode and a cathode piled one upon another on a substrate and the said light-emitting layer comprises a phosphorescent dopant and an indolocarbazole derivative as a host material. The indolocarbazole derivative is represented by the following formula (3) wherein Ar is an aromatic group and L is a direct bond or an aromatic group.Type: ApplicationFiled: April 30, 2009Publication date: March 10, 2011Applicant: NIPPON STEEL CHEMICAL CO., LTD.Inventors: Takahiro Kai, Masaki Komori, Toshihiro Yamamoto
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Publication number: 20110039803Abstract: Solid forms comprising a compound useful in the treatment, prevention and management of various conditions and diseases are provided herein. In particular, provided herein are solid forms comprising (2-carbamoyl-5-chloro-1H-indol-3-yl)-[3-((E)-2-cyano-vinyl)-5-methyl-phenyl]-(R)-phosphinic acid methyl ester, including salts thereof, having utility for the treatment, prevention and management of conditions and disorders including, but not limited to, human immunodeficiency virus infection.Type: ApplicationFiled: March 27, 2009Publication date: February 17, 2011Inventors: Adel M. Moussa, Mike H. O'Neill, Xiaohong Sheng
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Patent number: 7834215Abstract: The present invention is based on new ligand systems of the general formula (I). These ligand systems can be used advantageously in transition metal-catalyzed asymmetric syntheses. Likewise encompassed are the transition metal complexes thus prepared, a process for preparing the ligands and the use of the complexes in asymmetric synthesis.Type: GrantFiled: March 2, 2006Date of Patent: November 16, 2010Assignee: Evonik Degussa GmbHInventors: Jens Holz, Armin Boerner, Odalys Esperanza Zayas Vargas, Juan Jose Almena Perea, Axel Monsees, Renat Kadyrov, Thomas Riermeier
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Publication number: 20100179324Abstract: An anti-tumor agent containing, as an active ingredient, at least one of a sulphostin-related compound represented by the following General Formula (I), a pharmacologically acceptable salt thereof and a hydrate thereof; and a pharmaceutical composition containing the anti-tumor agent: where n is an integer of 1 to 3.Type: ApplicationFiled: January 11, 2010Publication date: July 15, 2010Applicants: Microbial Chemistry Research Foundation, NIPPON KAYAKU KABUSHIKI KAISHAInventors: Tetsuo AKIYAMA, Toru Masuda, Masatoshi Abe
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Publication number: 20100099875Abstract: The invention relates to novel organo phosphorus P-chiral optically active compounds of formula (I) having a hydroxyl, mercapto, amino, carboxyl, sulfonyl group on aryl near a phosphorus atom, to the preparation and the use thereof in then asymmetrical catalysis of unsaturated compounds. Novel acylphosphine optically pure ligands embodied in the form of transition metal complexes exhibit an increased activity and enantloselectivity, in particular in asymmetrical hydrogenation, in comparison with the same type Uganda such as DiPAMP.Type: ApplicationFiled: June 20, 2006Publication date: April 22, 2010Applicants: PHOSPHOENIX SARL, NATIONAL INSTITUTE OF CHEMISTRYInventors: Michel Stephan, Barbara Mohar
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Publication number: 20100024133Abstract: Tris(heterocyclyl)-metal complexes and the use thereof as bleach catalysts are described.Type: ApplicationFiled: October 12, 2009Publication date: February 4, 2010Applicant: Henkel AG & Co. KGaAInventors: Andre Hätzelt, Anette Nordskog, Stefan Leopold, Peter Schmiedel, Wolfgang von Rybinski, Jörg Sundermeyer, Jan Döring
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Publication number: 20090326243Abstract: The present invention relates to indolyl phosphine ligands, and methods of making such ligands utilizing phenyl hydrazines and aryl ketones as the starting material. The present invention further includes uses of the ligands in the synthesis of pharmaceuticals, materials, and agriculture.Type: ApplicationFiled: June 30, 2008Publication date: December 31, 2009Applicant: The Hong Kong Polytechnic UniversityInventors: Fuk Yee Kwong, Chau Ming So
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Patent number: 7625939Abstract: The present invention relates to DP IV-inhibitors of formula (1) for the treatment and/or prophylaxis of diseases of mammals including cancer and tumors, metastasis and tumor colonization; and metabolic diseases.Type: GrantFiled: May 14, 2008Date of Patent: December 1, 2009Assignee: Probiodrug AGInventors: Ulrich Heiser, Andre J. Niestroj, Ulf-Torsten Gaertner, Hans-Ulrich Demuth
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Publication number: 20090281330Abstract: The present invention involves new nitrons carrying a positive charge, useful in trapping of free radicals and especially the superoxide radical, of general formula:Type: ApplicationFiled: July 6, 2007Publication date: November 12, 2009Inventors: Paul Tordo, Jean-Pierre Bernard Finet, Florence Nathalie Laurence Chalier, Olivier Ouari, Micael Hardy
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Patent number: 7589081Abstract: The present invention relates to novel nitrogen-containing monodentate phosphane ligands of formula (I) and to their use in catalytic reactions, especially in the improvement of haloaromatic compounds.Type: GrantFiled: May 3, 2004Date of Patent: September 15, 2009Assignee: DEGUSSA GmbHInventors: Alexander Zapf, Mark Sundermeier, Ralf Jackstell, Matthias Beller, Thomas Riermeier, Axel Monsees, Uwe Dingerdissen
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Patent number: 7589215Abstract: The present invention relates to ligands of the general formula (I). In addition, a process for the production thereof and the use thereof are demonstrated.Type: GrantFiled: December 12, 2006Date of Patent: September 15, 2009Assignee: Degussa AGInventors: Armin Boerner, Jens Holz, Axel Monsees, Thomas Riermeier, Renat Kadyrov, Carsten A. Schneider, Uwe Dingerdissen, Karlheinz Drauz
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Publication number: 20090227801Abstract: The invention relates to chiral phosphorus chelate compounds, to catalysts comprising such a compound such a compound as the ligand, and to asymmetric synthesis methods in the presence of such a catalyst.Type: ApplicationFiled: October 10, 2005Publication date: September 10, 2009Applicant: BASF AKTIENGESELLSCHAFTInventors: Wolfgang Ahlers, Martina Egen, Martin Volland, Christoph Jakel, Frank Hettche, Rocco Paciello
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Publication number: 20090169475Abstract: Methods of imaging tissue of a mammal which expresses chymase include administering to the mammal an effective amount of a radiolabeled chymase inhibitor.Type: ApplicationFiled: December 18, 2008Publication date: July 2, 2009Inventors: John W. Babich, William C. Eckelman, John Joyal, Craig Zimmerman
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Publication number: 20090163444Abstract: 3-phosphoindole compounds for the treatment of retroviral infections, and particularly for HIV, are described. Also included are compositions comprising the 3-phosphoindole derivatives alone or in combination with one or more other anti-retroviral agents, processes for their preparation, and methods of manufacturing a medicament incorporating these compounds.Type: ApplicationFiled: November 21, 2008Publication date: June 25, 2009Inventors: Richard Storer, Cyril Dousson, Francois-Rene Alexandre, Arlene Roland
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Patent number: 7550406Abstract: Provided are a catalyst composition comprising a bidentate ligand, a monodentate ligand, and a transition metal catalyst and a process of hydroformylation of olefins, comprising reacting the olefin compound with gas mixture of hydrogen and carbon monoxide with stirring at an elevated pressure and temperature in the presence of the catalyst composition to produce aldehyde. The present catalytic compositions show high catalytic activity, high normal-to-iso aldehyde selectivity, and high stability.Type: GrantFiled: July 3, 2004Date of Patent: June 23, 2009Assignee: LG Chem. Ltd.Inventors: You Moon Jeon, Dong Hyun Ko, O Hak Kwon, Sung Shik Eom, Sang Gi Lee, Ji Joong Moon, Kwang Ho Park
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Patent number: 7531657Abstract: A method for preparing a compound represented by the following general formula (5) where, n is an integer of 0 to 3; and Y represents a protecting group for an amino group, the method including the steps of reacting a compound represented by the following general formula (3) where n and Y are as described above, with a silylating agent, and subsequently reacting it with P (?O) T3, where T represents a halogen atom, and further with ammonia.Type: GrantFiled: December 16, 2002Date of Patent: May 12, 2009Assignee: Nippon Kayaku Kabushiki KaishaInventors: Masashi Nagai, Hiroko Yamazaki, Keiichirou Yamamoto, Masatoshi Abe
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Patent number: 7511154Abstract: A process for producing the compound (1?benzyl-2-oxo-[1,3?]-(R)-bipyrrolidinyl-3-(R,S)-yl)-triphenyl-phosphonium bromide which is an intermediate for antibacterial vinylpyrrolidinone-cephalosporin derivatives.Type: GrantFiled: July 26, 2007Date of Patent: March 31, 2009Assignee: Basilea Pharmaceuticals AGInventor: Mark Rogers-Evans
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Publication number: 20080306264Abstract: The present invention concerns novel bidentante optionally N-containing P-ligands of general Formula (I) embracing a two-ring-system and processes for synthesizing them, transition metal complexes of these compounds and their use as catalysts.Type: ApplicationFiled: April 14, 2005Publication date: December 11, 2008Applicant: Degussa AGInventors: Renat Kadyrov, Juan Jose Almena Perea, Axel Monsees, Thomas Riermeier, Ilias Z. Ilaldinov
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Publication number: 20080269492Abstract: The invention relates to novel ionic compounds with low risk of combustion, more particularly, ionic compounds represented by the general formula (I): (NPR12)n . . . (I) [wherein R1?s are each independently halogeno or a monovalent substituent and at least one of R1?s is a ionic substituent represented by the general formula (II): —N+R23X? . . . (II) (wherein R2?s are each independently a monovalent substituent or hydrogen, with the proviso that at least one of R2?s is not hydrogen, or R2?s may be united to form a ring; and X? is a monovalent anion); and n is 3 to 15].Type: ApplicationFiled: October 12, 2006Publication date: October 30, 2008Applicant: BRIDGESTONE CORPORATIONInventors: Masashi Otsuki, Hiroshi Kanno
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Publication number: 20080200695Abstract: The present invention is based on new ligand systems of the general formula (I). These ligand systems can be used advantageously in transition metal-catalysed asymmetric syntheses. Likewise encompassed are the transition metal complexes thus prepared, a process for preparing the ligands and the use of the complexes in asymmetric synthesis.Type: ApplicationFiled: March 2, 2006Publication date: August 21, 2008Applicant: DEGUSSA GmbHInventors: Jens Holz, Armin Boerner, Odalys Esperanza Zayas Vargas, Juan Jose Almena Perea, Axel Monsees, Renat Kadyrov, Thomas Riermeier
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Patent number: 7348318Abstract: There are disclosed a novel ?-amino-N-(diaminophosphinyl)lactam derivative represented by general formula (1): wherein, for example, A is a hydrogen atom or a substituent such as a lower alkyl group or the like; W, X, Y and Z are independently a hydrogen atom or a substituent such as a lower alkyl group, aryl group, arylacyl group, arylaminocarbonyl group or the like; and Q is —(CH2)n— wherein n is 0 to 3, or its salt, and a therapeutic agent and a prophylactic agent for myelosuppression, a therapeutic agent for infectious diseases, an agent for increasing the number of leukocytes and a dipeptidyl peptidase IV inhibitor which comprise the above-mentioned derivative or salt thereof as an active ingredient.Type: GrantFiled: March 24, 2003Date of Patent: March 25, 2008Assignees: Nippon Kayaku Kabushiki Kaisha, Zaidan Hojin Biseibutsu Kagaku Kenkyu KaiInventors: Masatoshi Abe, Masashi Nagai, Keiichirou Yamamoto, Chihiro Nishimura
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Publication number: 20080009636Abstract: The present invention involves new nitrons carrying a positive charge, useful in trapping of free radicals and especially the superoxide radical, of general formula:Type: ApplicationFiled: October 24, 2006Publication date: January 10, 2008Inventors: Paul Tordo, Jean-Pierre Bernard Finet, Florence Nathalie Laurence Chalier, Olivier Ouari, Micael Hardy
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Patent number: 7307037Abstract: Metallic catalysts of the general formula (I) and their precursors, suitable for chemo- regio- and stereoselective reactions, derived from ortho-bis-(1-phospholanyl)-heteroarenes.Type: GrantFiled: March 3, 2003Date of Patent: December 11, 2007Assignee: Chemi S.p.A.Inventors: Francesco Sannicolo′, Oreste Piccolo, Tiziana Benincori, Mara Sada, Alessandra Verrazzani, Simona Tollis, Elio Ullucci, Lorenzo De Ferra, Simona Rizzo
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Patent number: 7247640Abstract: A medicament for prophylaxis or treatment of bone marrow suppression, for treatment of infectious diseases and for increasing the number of leukocytes, which comprise as an active ingredient a sulphostin-related compound represented by general formula (I): wherein n is an integer of 0 to 3, or a pharmacologically acceptable salt thereof.Type: GrantFiled: July 22, 2005Date of Patent: July 24, 2007Assignees: Nippon Kayaku Kabushiki Kaisha, Zaidan Hojin Biseibutsu Kagaku Kenkyu KaiInventors: Takumi Yamashita, Chihiro Nishimura, Tetsushi Saino, Yasuhiko Muraoka, Tomio Takeuchi
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Patent number: 7173138Abstract: Pnicogen chelate compounds which have two pnicogen-containing groups joined to one another via a xanthene-like or triptycene-like molecular skeleton and in which at least one pyrrole group is covalently bound via its nitrogen atom to each pnicogen atom form complexes with metals of transition group VIII which are useful as catalysts for the hydroformylation of olefins.Type: GrantFiled: March 28, 2002Date of Patent: February 6, 2007Assignee: BASF AktiengesellschaftInventors: Wolfgang Ahlers, Rocco Paciello, Dieter Vogt, Peter Hofmann
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Patent number: 7105556Abstract: Compounds are provided which have the structure wherein Q is C or N, X1 is C or N, and R1, R2, R2a, R2b, R2c, R3, Y, A, m, n, X2, X3 and X4 are as defined herein, which compounds are useful as antidiabetic, hypolipidemic, and antiobesity agents.Type: GrantFiled: May 22, 2002Date of Patent: September 12, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Peter T. Cheng, Yoon Jeon, Wei Wang
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Patent number: 7094907Abstract: The invention relates to a process for the manufacture of bidentate ligands of the formula IA and IIA, characterized in that N,N-(optionally substituted)dialkylamino phosphines bound to an aromatic carbon are lithiated in ortho-position and the lithiated compounds are further converted to said bidentate ligands: wherein X1 is NR, O or S; X2 is CHR1 or CR1; X3 is CHR2 or NR2, or, if X2is CR1, X3 is CR2 or N; and R, R1 and R2 are radicals such as alkyl groups or R1 and R2 together form an annealed ring; Y1*, Y2* and Y1?* are, independently of each other, an element of the fifth group of the periodic table of elements as such or in thioxo or oxo form; Z1*, Z2*, Z3*, Z4*, Z1?*, Z2?* are, independently of each other, for example halogen, hydrogen, or an unsubstituted or substituted moiety selected from radicals such as alkyl groups; the substituents have otherwise the meanings given in the specification; and the ligands are capable of forming metal complexes, which can be used as catalysts in stereoselective sType: GrantFiled: October 2, 2002Date of Patent: August 22, 2006Assignee: Solvias AGInventor: Ulrich Berens
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Patent number: 7081536Abstract: The invention relates to novel ligands of the phosphanylbenzothiophenyl-dihydroisoxazoline, phosphanyl-dihydrooxazolyl-indole and phosphanyl-dihydrooxazolyl-benzofuran type, especially compounds of formula I and mixtures of such compounds, wherein X is oxygen, sulfur, selenium or NQ, wherein Q is unsubstituted or substituted aryl, or alkyl or substituted alkyl; n is 0, 1, 2, 3 or 4; A1 and A2 are each an organic radical capable of bonding to phosphorus, especially unsubstituted or substituted alkyl, unsubstituted or substituted aryl, unsubstituted or substituted heterocyclyl, unsubstituted or substituted cycloalkyl, or —N(D)2 wherein D2 is alkyl or substituted alkyl; or A1 and A2 together with the bonding phosphorus atom form a ring, which may be unsubstituted or substituted; Y, Y?, Y? and Y?? are each independently of the other hydrogen or alkyl, substituted alkyl, unsubstituted or substituted aryl, or unsubstituted or substituted heterocyclyl, at least one of the radicals Y, Y?, Y? or Y?? being one ofType: GrantFiled: August 1, 2002Date of Patent: July 25, 2006Assignee: Ciba Specialty Chemicals CorporationInventors: Nicole End, Catherine Stoessel, Ulrich Berens, Pier Giorgio Cozzi
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Patent number: 6902586Abstract: The present invention relates to the use for dyeing keratin fibers, in particular human keratin fibers such as the hair, of a dye precursor bearing at least one phosphate substituent of formula —O—PO(OH)2, in the presence of at least one acid or alkaline phosphatase.Type: GrantFiled: July 2, 2002Date of Patent: June 7, 2005Assignee: L'OrealInventors: Rui Pereira, Richard Martin
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Patent number: 6900238Abstract: Combinatorial libraries of HIV and FIV protease inhibitors are characterized by ?-keto amide or hydroxyethylamine core structures flanked by on one side by substituted pyrrolidines, piperidines, or azasugars and on the other side by phenylalanine, tyrosine, or substituted tyrosines. The libraries are synthesized via a one step coupling reaction. Highly efficacious drug candidates are identified by screening the libraries for binding and inhibitory activity against both HIV and FIV protease. Drug candidates displaying clinically useful activity against both HIV and FIV protease are identified as being potentially resistive against a loss of inhibitory activity due to development of resistant strains of HIV.Type: GrantFiled: December 9, 1996Date of Patent: May 31, 2005Assignee: The Scripps Research InstituteInventors: Chi-Huey Wong, Deborah H. Slee, Karen Laslo
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Patent number: 6828442Abstract: A new process is disclosed for the preparation of bipyrrolidinyl compounds of formula I wherein * signifies an asymmetric center with an (R) or (S) configuration and X represents chlorine, bromine or iodine. The compounds of formula I are important building blocks for the production of useful products in the chemical and in the pharmaceutical industry. In particular they are useful for the production of antibacterial substances such as vinylpyrrolidinone-cephalosporin derivatives.Type: GrantFiled: February 14, 2003Date of Patent: December 7, 2004Assignee: Basilea Pharmaceutica AGInventor: Mark Rogers-Evans
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Publication number: 20040138495Abstract: The invention relates to solid phase processes for the systematic preparation of chemical compounds from the group of the phosphonous or phosphinic acids and/or derivatives thereof and the corresponding substance libraries which can be employed for test purposes, in particular tests for biological activity.Type: ApplicationFiled: December 17, 2003Publication date: July 15, 2004Inventors: Klaus Haaf, Marcel Patek
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Publication number: 20040116713Abstract: N-Phenylpyrrolebisphosphines of the formula I 1Type: ApplicationFiled: January 20, 2004Publication date: June 17, 2004Inventors: Matthias Beller, Ralf Jackstell, Holger Klein, Detlef Heller, Hans-Joachim Drexler, Klaus-Diether Wiese, Dirk Rottger
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Publication number: 20040116702Abstract: The invention relates to acyl- or bisacylphosphine derivatives according to formula (1), wherein: Y represents O, S, NR3, N—OR3 or N—NR3R54; Z represents O, S, NR3, N—OR3, N—NR3R4 or a free electron pair; Het1 and Het2, independent of one another, represent O, S and/or NR5, and; the other radicals have the meanings as cited in the description. The invention also relates to methods for producing these derivatives and to the use thereof.Type: ApplicationFiled: October 14, 2003Publication date: June 17, 2004Inventors: Ralf Noe, Andreas Henne, Matthias Maase
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Publication number: 20040077605Abstract: Fused cyclic compounds, methods of using such compounds in the treatment of nuclear hormone receptor-associated conditions such as cancer and immune disorders, and pharmaceutical compositions containing such compounds.Type: ApplicationFiled: December 18, 2002Publication date: April 22, 2004Inventors: Mark E. Salvati, James Aaron Balog, Dacia A. Pickering, Soren Giese, Aberra Fura, Wenying Li, Ramesh N. Patel, Ronald L. Hanson, Toomas Mitt, Jacques Y. Roberge, James R. Corte, Steven H. Spergel, Richard A. Rampulla, Raj N. Misra, Hai-Yun Xiao
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Publication number: 20040039189Abstract: The invention relates to novel amidite derivatives and their use as linker units for synthesizing polymers, especially biopolymers such as nucleic acids, peptides and saccharides, on the surface of solid supports. Use of the linker derivatives of the invention makes it possible to regenerate the surfaces without damage.Type: ApplicationFiled: July 30, 2003Publication date: February 26, 2004Inventors: Ramon Guimil, Matthias Scheffler
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Publication number: 20030232991Abstract: Chiral ligands and transition metal complexes based on such chiral ligands useful in asymmetric catalysis are disclosed. The chiral ligands include (R,S,S,R)-DIOP*. The ruthenium complex reduces enamide to the corresponding amine with up to 99% enantioselectivity. The transition metal complexes of the chiral ligands are useful in asymmetric reactions such as asymmetric hydrogenation, hydride transfer, hydrosilylation, hydroboration, hydrovinylation, hydroformylation, hydrocarboxylation, isomerization, allylic alkylation, cyclopropanation, Diels-Alder reaction, Heck reaction, isomerization, Aldol reaction, Michael addition and epoxidation reactions.Type: ApplicationFiled: April 10, 2003Publication date: December 18, 2003Applicant: The Penn State Research FoundationInventor: Xumu Zhang
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Publication number: 20030225284Abstract: A scalable process for purification of phosphorodiamidite includes steps of solubilizing a crude phosphorodiamidite in an apolar organic solvent, contacting the non-polar organic solvent with a polar phase comprising a polar organic solvent to remove impurities from the solubilized phosphorodiamidite, and removing the non-polar organic solvent from the phosphorodiamidite.Type: ApplicationFiled: April 11, 2002Publication date: December 4, 2003Inventors: Quanlai Song, Bruce Ross