Phosphorus Attached Directly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 546/21)
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Publication number: 20110251390Abstract: Chiral amino alcohol and amino phosphine compounds are provided herein, which compounds are useful for asymmetric synthesis.Type: ApplicationFiled: October 2, 2009Publication date: October 13, 2011Inventors: Daniel L. Comins, Sonja S. Capracotta
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Publication number: 20110195933Abstract: The invention encompasses pyrazolo[1,5-a]pyridine derivatives which selectively inhibit microtubule affinity regulating kinase (MARK) and are therefore useful for the treatment or prevention of Alzheimer's disease. Pharmaceutical compositions and methods of use are also included.Type: ApplicationFiled: July 27, 2009Publication date: August 11, 2011Inventors: Jason D. Katz, Sandra L. Knowles, James P. Jewell, David L. Sloman, Matthew G. Stanton, Njamkou Noucti
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Publication number: 20110172423Abstract: An organic light-emitting diode comprising at least one cyclic phosphazene compound, a light-emitting layer formed from at least one matrix material and at least one emitter material, wherein the at least one matrix material comprises at least one cyclic phosphazene compound, the use of cyclic phosphazene compounds in organic light-emitting diodes and a device selected from the group consisting of stationary visual display units, mobile visual display units and illumination units comprising at least one inventive organic light-emitting diode, and selected cyclic phosphazene compounds and processes for preparing them.Type: ApplicationFiled: June 17, 2009Publication date: July 14, 2011Applicants: BASF SE, KONINKLIJKE PHILIPS ELECTRONICS N.V., OSRAM OPTO SEMICONDUCTORS GMBHInventors: Evelyn Fuchs, Oliver Molt, Nicolle Langer, Christian Lennartz, Peter Strohriegl, Pamela Schroegel, Herbert Friedrich Boerner, Volker Van Elsbergen, Arvid Hunze, Ralf Krause
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Patent number: 7863447Abstract: A compound of the formula I or I?, where the radicals R1 are each, independently of one another, a hydrogen atom or C1-C4-alkyl and R?1 is C1-C4-alkyl; X1 and X2 are each, independently of one another, a sec-phosphino group; R2 is (1) hydrogen, (2) R01R02R03Si—, (3) C1-C18-acyl substituted with halogen, hydroxyl, C1-C8-alkoxy or R04R05N—, or (4) R06—X01—C(O)—; R01, R02 and R03 are each, independently of one another, C1-C12-alkyl, unsubstituted or C1-C4-alkyl- or C1-C4-alkoxy-substituted C6-C10-aryl or C7-C12-aralkyl; R04 and R05 are each, independently of one another, hydrogen, C1-C12-alkyl, C3-C8-cycloalkyl, C6-C10-aryl or C7-C12-aralkyl, or R04 and R05 together are trimethylene, tetramethylene, pentamethylene or 3-oxapentylene; R06 is C1-C18-alkyl, unsubstituted or C1-C4-alkyl- or C1-C4-alkoxy-substituted C3-C8-cycloalkyl, C6-C10-aryl or C7-C12-aralkyl; X01 is —O— or —NH—; T is C-bonded C3-C20-heteroarylene; v is 0 or an integer from 1 to 4; X1 in the heteroring of the heteroarylene is bound in the orthType: GrantFiled: April 19, 2006Date of Patent: January 4, 2011Assignee: Umicore AG & Co., KGInventors: Martin Kesselgruber, Marc Thommen, Matthias Lotz
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Patent number: 7851701Abstract: A photoelectric conversion device using a semiconductor fine material such as a semiconductor fine particle sensitized with a dye carried thereon, characterized in that the dye is a methine type dye having a specific partial structure, for example, a methine type dye having a specific carboxyl-substituted hetero ring on one side of a methine group and an aromatic residue substituted with a dialkylamino group or an organic metal complex residue on the other side of the methine group, or a methine type dye having a carboxyl-substituted aromatic ring on one side of a methine group and a heteroaromatic ring having a dialkylamino group or an organic metal complex residue on the other side of the methine group; and a solar cell using the photoelectric conversion element. The photoelectric conversion element exhibits a conversion efficiency comparable or superior to that of a conventionally known photoelectric conversion element sensitized with a methine type dye.Type: GrantFiled: July 5, 2002Date of Patent: December 14, 2010Assignee: Nippon Kayaku Kabushiki KaishaInventors: Masaaki Ikeda, Koichiro Shigaki, Teruhisa Inoue
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Publication number: 20100298271Abstract: Compound of Formula I or a salt thereof for treating cancer, wherein X represents CH or N; R1 represents hydrogen or —CH2COR5; R5 represents hydroxy, optionally hydroxylated alkoxy, amino or alkylamido; R2 represents ZYR6; Z represents a bond, or a C1-3 alkylene or oxoalkylene group optionally substituted by R7; Y represents a bond, an oxygen atom or NR6; R6 is a hydrogen atom, COOR8, an alkyl, alkenyl, cycloalkyl, aryl or aralkyl group optionally substituted by one or more selected from COOR8, CONR82, NR82, OR8, ?NR8, ?O, OP(O)(OR8)R7 and OSO3M; R7 is hydroxy, an optionally hydroxylated, optionally alkoxylated alkyl or aminoalkyl group; R8 is a hydrogen atom or an optionally hydroxylated, optionally alkoxylated alkyl group; M is a hydrogen atom or one equivalent of a physiologically tolerable cation; R3 represents C1-8 alkylene, 1,2-cykloalkylene, or 1,2-arylene, optionally substituted with R7; and R4 represents hydrogen or C1-3 alkyl.Type: ApplicationFiled: December 12, 2008Publication date: November 25, 2010Applicant: PLEDPHARMA ABInventors: Jan Olof G. Karlsson, Tino Kurz, Rolf Andersson
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Patent number: 7812251Abstract: A photosensitizing transition metal complex of the formula (Ia) MLY1, (Ib) MLX3 (Ic) MLY2X, (Id) MLY3X or (Ie) MLY4X in which M is a transition metal selected from ruthenium, osmium, iron, rhenium and technetium, preferably ruthenium or osmium. X is a co-ligand independently selected from NCS—, Cl—, Br—, I—, CN—, H2O; pyridine unsubstituted or substituted by at least one group selected from vinyl, primary, secondary or tertiary amine, OH and C1-30 alkyl, preferably NSC and CN—; L is a tridentate polypyridine ligand, carrying at least one carboxylic, phosphoric acid or a chelating group and one substituted or unsubstituted alkyl group having 1 to 50 carbon atoms, substituted or unsubstituted alkylamide group having 2 to 30 carbon atoms or substituted or unsubstituted aralkyl group having 7 to 50 carbon atoms.Type: GrantFiled: October 15, 2004Date of Patent: October 12, 2010Assignee: Sharp Kabushiki KaishaInventors: Ashraful Islam, Liyuan Han, Atsushi Fukui
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Publication number: 20100240896Abstract: The present invention relates to a process for the hydroformylation of compounds of the formula (I), where X is C, P(Rx), P(O—Rx) S or S(?O), where Rx is H, alkyl, cycloalkyl, heterocycloalkyl, aryl or hetaryl; A is a divalent bridging group having from 1 to 4 bridging atoms; and R1 is H, alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl or hetaryl; or salts thereof; in which the compound of the formula (I) is reacted with carbon monoxide and hydrogen in the presence of a catalyst comprising a complex of a metal of transition group VIII with a compound of the formula (II), where Pn is a pnicogen atom; W is a divalent bridging group having from 1 to 8 bridging atoms; R2 is a functional group capable of forming an intermolecular, noncovalent bond with the group —X(?O)OH; R3, R4 are each alkyl, cycloalkyl, heterocycloalkyl, aryl or hetaryl; a, b, c are each 0 or 1; and Y1, Y2 and Y3 are each O, S, NRa or SiRbRc; and also compounds of the formula (II.Type: ApplicationFiled: November 4, 2008Publication date: September 23, 2010Applicant: BASF SEInventors: Jens Rudolph, Joachim Schmidt-Leithoff, Rocco Paciello, Bernhard Breit, Tomas Smejkal
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Publication number: 20100227978Abstract: The present invention relates to new types of metal complexes. Such compounds can be used as active components (=functional materials) in a series of different types of applications which can be classed within the electronics industry in the widest sense. The inventive compounds are described by the structure 1 and the formulae (1) to (60).Type: ApplicationFiled: May 18, 2010Publication date: September 9, 2010Applicant: Merck Patent GmbHInventors: Philipp Stoessel, Hubert Spreitzer
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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: 20100174079Abstract: Disclosed is a process for producing an optically active phosphorus compound having an R- or S-type absolute configuration on phosphorus in a simple manner and at high efficiency, while avoiding racemization. An optically active phosphorus compound having an R- or S-type absolute configuration on phosphorus represented by the general formula (III) can be produced by reacting an optically active phosphorus compound having an R- or S-type absolute configuration on phosphorus represented by the general formula (I) with a metal compound represented by the general formula (II) and water. (I) wherein R1 represents a hydrogen atom, analkyl group, a cycloalkyl group, an aralkyl group or an aryl group; and R2 represents a hydrogen, an alkyl group, a cycloalkyl group, an aryl group, an aralkyl group, alkenyl group, an alkoxy group, an aryloxy group, a heterocyclic ring residue or a silyl-containing group. R3M (II) wherein R3 is the same as R2; and M represents a lithium or magnesium halide MgX (X?Cl, Br or I).Type: ApplicationFiled: August 20, 2007Publication date: July 8, 2010Applicant: National Institute of Advanced Industrial Science TechnologyInventors: Li-Biao Han, Qing Xu
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Patent number: 7723330Abstract: Compounds of Formulas Ia and Ib, and stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting receptor tyrosine kinases and for treating disorders mediated thereby. Methods of using compounds of Formula Ia and Ib, and stereoisomers, geometric isomers, tautomers, solvates and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.Type: GrantFiled: March 6, 2007Date of Patent: May 25, 2010Assignees: Array BioPharma Inc., Genentech, Inc.Inventors: James F. Blake, Steven Armen Boyd, Jason De Meese, Kin Chiu Fong, John J. Gaudino, Tomas Kaplan, Allison L. Marlow, Jeongbeob Seo, Allen A. Thomas, Hongqi Tian, Frederick Cohen, Wendy B. Young
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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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Patent number: 7700777Abstract: The invention provides crystalline forms of biphenyl-2-ylcarbamic acid 1-(2-{[4-(4-carbamoylpiperidin-1-ylmethyl)benzoyl]methylamino}ethyl)piperidin-4-yl ester, and pharmaceutically acceptable solvates thereof. The crystalline form can be a freebase, or a salt such as a diphosphate, monosulfate or dioxalate salt. The invention also provides pharmaceutical compositions comprising these crystalline compounds or prepared using these compounds; processes and intermediates for preparing the crystalline compounds; and methods of using these compounds to treat a pulmonary disorder.Type: GrantFiled: August 8, 2007Date of Patent: April 20, 2010Assignee: Theravance, Inc.Inventors: Sabine Axt, Timothy J. Church
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Publication number: 20100036127Abstract: A process for preparing the S or R enantiomer of a compound of formula A, the process comprising subjecting a compound of formula B to asymmetric hydrogenation in the presence of a chiral catalyst and a source of hydrogen, wherein: X is CH2, oxygen or sulphur; R1, R2 and R3 are the same or different and signify hydrogens, halogens, alkyl, alkyloxy, hydroxy, nitro, alkylcarbonylamino, alkylamino or dialkylamino group; and R4 is alkyl or aryl, wherein: the term alkyl means hydrocarbon chains, straight or branched, containing from one to six carbon atoms, optionally substituted by aryl, alkoxy, halogen, alkoxycarbonyl or hydroxycarbonyl groups; the term aryl means a phenyl or naphthyl group, optionally substituted by alkyloxy, halogen or nitro group; and the term halogen means fluorine, chlorine, bromine or iodine.Type: ApplicationFiled: December 12, 2007Publication date: February 11, 2010Applicant: BIAL-PORTELA & CA, S.A.Inventors: David Alexander Learmonth, Antonio Zanotti-Gerosa, Gabriela Alexandra Grasa, Alexander Beliaev
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Publication number: 20090326226Abstract: The present invention relates to a process for asymmetric synthesis in the presence of a chiral catalyst comprising at least one complex of a metal of transition group VIII with ligands capable of dimerization via noncovalent bonds, such catalysts and their use.Type: ApplicationFiled: September 24, 2008Publication date: December 31, 2009Applicant: BASF AKTIENGESELLSCHAFTInventors: Christoph Jakel, Martin Volland, Thomas Mackewitz, Rocco Paciello, Bernhard Breit, Wolfgang Seiche, Martine Weis, Christoph Waloch
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Publication number: 20090299048Abstract: This invention features bis-amides of pyrophosphoric acid and bisphosphonic acids, their preparation, and their use in synthesis of P1,P4-dinucleoside tetraphosphates, tetraphosphonates, and related compounds.Type: ApplicationFiled: July 23, 2007Publication date: December 3, 2009Applicant: GLSynthesis IncInventors: Ivan Yanachkov, George E. Wright
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Publication number: 20090281060Abstract: Compounds of Formula (I), R1-A-V—B—R2; or pharmaceutically acceptable salts thereof, are agonists of GPR116 and are useful as regulators of satiety, e.g. for the treatment of obesity, and for the treatment of diabetes.Type: ApplicationFiled: December 23, 2004Publication date: November 12, 2009Applicant: PROSIDION LIMITEDInventors: Matthew Fyfe, John King-Underwood, Lisa Sarah Bertram (Gardner), Gerard Hugh Thomas, Martin Procter, Chrystelle Rasamison, Karen Schofield
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Publication number: 20090270623Abstract: A compound (8) represented by the formula: (8) wherein R1 represents a 6- to 14-membered aromatic hydrocarbon ring group which may have a substituent; and n represents 0 to 2, can be produced with good efficiency by reacting a compound (3) represented by the formula: (3) wherein R1 and n are as defined above; and Q represents a single bond or —CH(Y)— where Y represents a hydrogen atom or a C1-6 alkyl group] with 3-methoxy-4-(4-methyl-1H-imidazol-1-yl)benzaldehyde in the presence of a base.Type: ApplicationFiled: November 17, 2006Publication date: October 29, 2009Inventors: Naoyuki Shimomura, Nobuaki Sato, Toshihiko Kaneko, Mamoru Takaishi, Kazunori Wakasugi, Seiji Yoshikawa, Yoshihiro Nishikawa, Taiju Nakamura, Tohru Fukuyama
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Patent number: 7563782Abstract: There is provided a T-type calcium channel blocker that is optically active 1,4-dihydropyridine compound, a pharmaceutically acceptable salt thereof or a solvate thereof, of formula (1) wherein R1 and R2 are independently of each other C1-6 alkyl group or R1 and R2 together form —CR5R6—CR7R8, —CR5R6—CR7R8—CR9R10— or —CR5R6—CR7R8—CR9R10—CR11R12—, etc., X1 and X2 are independently of each other O or NR13, Ar is optionally substituted phenyl group, etc., Ra and Rb are independently of each other C1-6alkyl group, —L2—NR16R17, CH2O—L2—NR16R17CN, —L2—N(CH2CH2)2NR16 or NR16R17, etc., Y is C1-20 alkyl group, —L3—NR18R19 and * is absolute configuration of R.Type: GrantFiled: March 29, 2004Date of Patent: July 21, 2009Assignee: Nissan Chemical Industries, Ltd.Inventors: Yukinori Masuda, Taiji Furukawa
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Patent number: 7560555Abstract: A process for the preparation of a compound of formula R1—Y1—P(NR2R3)2 is provided. The process comprises reacting a compound of formula PX3 with a compound of formula HNR2R3 to form a compound of formula X—P(NR2R3)2; and reacting the compound of formula X—P(NR2R3)2 with a compound of formula R1—Y1—H in the presence of a hydrocarbon solvent to form the compound of formula R1—Y1—P(NR2R3)2. R1 represents a phosphorus protecting group; R2 and R3 each independently represent an alkyl, prefer-ably a C1-6alkyl, group, or R2 and R3 are joined, together with the N to which they are attached, to form a 5-7 membered ring; Y1 represents O or S, preferably O; and X represents a halogen, preferably Cl. The preferred solvent is toluene.Type: GrantFiled: December 16, 2003Date of Patent: July 14, 2009Assignee: Avecia Biotechnology Inc.Inventors: Jonathan Mark Hardy, Stephen Edward Dinizo
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Publication number: 20090142672Abstract: The present invention provides an optical recording composition comprising a compound denoted by general formula (I) and a holographic recording medium comprising a recording layer, wherein the recording layer comprises a compound denoted by general formula (I). In general formula (I), each of R1, R2, and R3 independently denotes an alkyl group, aryl group, or heterocyclic group, X denotes an oxygen atom or sulfur atom, and n denotes 0 or 1.Type: ApplicationFiled: November 21, 2008Publication date: June 4, 2009Applicant: FUJIFILM CorporationInventor: Satoru YAMADA
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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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Publication number: 20090105279Abstract: The invention is related to compounds of Formula I: or a pharmaceutically acceptable salt, solvate, ester, and/or phosphonate thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.Type: ApplicationFiled: July 19, 2007Publication date: April 23, 2009Inventors: Carina E. Cannizzaro, James M. Chen, Manoj C. Desai, Michael L. Mitchell, Sundaramoorthi Swaminathan, Lianhong Xu, Zheng-Yu Yang
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Publication number: 20090081158Abstract: Provided herein are phosphadiazine polymerase inhibitor, for example, of any of Formulas IV, IV?, I?, II?, or IVa, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.Type: ApplicationFiled: August 27, 2008Publication date: March 26, 2009Applicant: Idenix Pharmaceuticals, Inc.Inventors: Cyril Dousson, Dominique Surleraux, Jean-Laurent Paparin, Claire Pierra, Arlene Roland
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Publication number: 20090018106Abstract: The present invention provides a lyophilized formulation of pyridoxal 5?-phosphate and a method of making the same. The present invention also provides an injectable formulation of pyridoxal 5?-phosphate reconstituted from the lyophilized formulation. The present invention further provides uses of the lyophilized and injectable formulations.Type: ApplicationFiled: March 30, 2006Publication date: January 15, 2009Applicant: Medicure International Inc.Inventor: Albert Friesen
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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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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: 20080009465Abstract: Compounds are provided which are phosphonate and phosphinate activators and thus are useful in treating diabetes and related diseases and have the structure wherein is a heteroaryl ring; R4 is —(CH2)n-Z-(CH2)m—PO(OR7)(OR8), —(CH2)nZ-(CH2)m—PO(OR7)Rg, —(CH2)n-Z-(CH2)m—OPO(OR7)Rg, —(CH2)nZ—(CH2)m—OPO(R9)(R10), or —(CH2)nZ—(CH2)m—PO(R9)(R10); R5 and R6 are independently selected from H, alkyl and halogen; Y is R7(CH2)s or is absent; and X, n, Z, m, R4, R5, R6, R7, and s are as defined herein; or a pharmaceutically acceptable salt thereof. A method for treating diabetes and related diseases employing the above compounds is also provided.Type: ApplicationFiled: June 28, 2007Publication date: January 10, 2008Inventors: Denis E. Ryono, Peter T.W. Cheng, Scott A. Bolton, Sean Chen, Yan Shi, Wei Meng, Joseph A. Tino, Hao Zhang, Richard B. Sulsky
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Patent number: 7253154Abstract: The invention relates to compounds of the following formula (I) or their salts: in which R1 represents OR4 or others, in which R4 is an alkyl group having 1-8 carbon atoms which may have a substituent or the like; R2 is halogen, nitro, cyano, carboxyl, or the like; R3 is hydrogen, halogen, hydroxyl, amino, carboxyl, or the like; X is NR11, oxygen, or sulfur, in which R11 is hydrogen, or an alkyl group having 1-8 carbon atom which may have a substituent; and each of Y and Z is CR12 or nitrogen, in which R12 has the same meaning as R3 above, and a xanthine oxidase inhibitor containing the compound as an active ingredient.Type: GrantFiled: November 14, 2002Date of Patent: August 7, 2007Assignee: Nippon Chemiphar Co., Ltd.Inventors: Shinichi Yoshida, Atsushi Tendo, Kunio Kobayashi, Nobutaka Mochiduki, Tomio Yamakawa, Yoriko Shinohara
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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: 7241745Abstract: The invention relates to a new pyridyl alkene and pyridyl alkine acid amides according to the general formula (I) as well as methods for their production, medicaments containing these compounds as well as their medical use, especially in the treatment of tumors or for immunosuppression.Type: GrantFiled: August 5, 2002Date of Patent: July 10, 2007Assignee: Astellas Pharma GmbHInventors: Elfi Biedermann, Max Hasmann, Roland Löser, Benno Rattel, Friedemann Reiter, Barbara Schein, Klaus Seibel, Klaus Vogt
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Patent number: 7081533Abstract: The present invention concerns novel unsymmetrical chiral diphosphines of a mixed aliphatic-aromatic type and processes for synthesizing them, complexes of these compounds and their use as catalysts.Type: GrantFiled: August 17, 2001Date of Patent: July 25, 2006Assignee: Degussa AGInventors: Boris E Bosch, Axel Monsees, Uwe Dingerdissen, Paul Knochel, Eike Hupe
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Patent number: 7074820Abstract: There is provided compounds of formula I, wherein R1, R2, R3, Y, n and B have meanings given in the description which are useful as competitive inhibitors of trypsin-like proteases, such as thrombin, and in particular in the treatment of conditions where inhibition of thrombin is required (e.g. thrombosis) or as anticoagulants.Type: GrantFiled: April 23, 2001Date of Patent: July 11, 2006Assignee: AstraZeneca ABInventor: Thomas Antonsson
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Patent number: 7063903Abstract: The present invention is generally directed to luminescent lanthanide compounds with phosphine oxide, phosphine oxide-sulfide, pyridine N-oxide, and phosphine oxide-pyridine N-oxide ligands. It also relates to electronic devices in which the active layer includes a lanthanide complex.Type: GrantFiled: December 14, 2004Date of Patent: June 20, 2006Assignee: E. I. du Pont de Nemours and CompanyInventors: Vladimir Grushin, Norman Herron, Viacheslav A. Petrov, Nora Sabina Radu, Ying Wang
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Patent number: 6919322Abstract: Novel FBPase inhibitors of the formula I are useful in the treatment of diabetes and other conditions associated with elevated blood glucose.Type: GrantFiled: March 7, 2001Date of Patent: July 19, 2005Assignee: Metabasis Therapeutics, Inc.Inventors: Brett C. Bookser, Qun Dang, K. Raja Reddy
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Patent number: 6875523Abstract: The present invention is generally directed to luminescent lanthanide compounds with phosphine oxide, phosphine oxide-sulfide, pyridine N-oxide, and phosphine oxide-pyridine N-oxide ligands. It also relates to electronic devices in which the active layer includes a lanthanide complex.Type: GrantFiled: June 27, 2002Date of Patent: April 5, 2005Assignee: E. I. du Pont de Nemours and CompanyInventors: Vladimir Grushin, Norman Herron, Viacheslav Alexandrovich Petrov, Nora Sabina Radu, Ying Wang
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Patent number: 6825211Abstract: The present invention provides bicyclic metabotropic glutamate receptor ligands, as well as compositions comprising such ligands, and methods for their use.Type: GrantFiled: August 20, 2003Date of Patent: November 30, 2004Assignee: Georgetown UniversityInventors: Alan P. Kozikowski, Darryl Hugh Steensma, Werner Tueckmantel, Gian Luca Araldi
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Publication number: 20040171587Abstract: The invention provides novel pyridines, pharmaceutical compositions comprising such pyridines, and the use of such compositions in treating injured mammalian nerve tissue, including but not limited to an injured spinal cord. in one embodiment, the compounds, compositions, and methods of the instant invention treat a mammalian nerve tissue injury by restoring action potential or nerve impulse conduction through a nerve tissue lesion. Significantly, in vivo application of compounds of the instant invention established, on the basis of SSEP testing, that the compounds provide longer lasting effects at lower concentrations than comparable treatment with the known agent 4-aminopyridine (4 AP).Type: ApplicationFiled: December 5, 2003Publication date: September 2, 2004Inventors: Richard B. Borgens, Riyi Shi, Stephen R. Byrn, Daniel T. Smith
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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: 20040126763Abstract: Exploitation of suitably functionalized heterocyclic molecules, in the design and synthesis of Fluorescence Resonance Energy Transfer (FRET) cassettes and their corresponding dideoxynucleotide terminators culminated into efficient reagents for DNA sequencing. Additionally, these FRET cassettes/terminators, of the present invention, derived from different classes of heterocyclic systems have high potential to be used for general labelling of biological molecules to generate highly sensitized signals. Their preparation, energy transfer efficiency, and use as labels, specifically, in DNA sequencing reactions is disclosed.Type: ApplicationFiled: December 20, 2002Publication date: July 1, 2004Inventors: Satyam Nampalli, Weihong Zhang, Sudhakar Rao, Shiv Kumar
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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: 20040116673Abstract: A novel class of compounds, i.e., 1,1-bis-H-phosphinates (or 1,1-bis-H-phosphinic acid derivatives) are provided. Also provided are novel methods for producing 1,1-bis-H-phosphinates and 1,1-bis-H-phosphinate conjugates. These compounds and conjugates are used as precursors of bisphosphonates and bisphosphonate conjugates, respectively, or as prodrugs directly for treating bone-related and various other diseases.Type: ApplicationFiled: December 13, 2002Publication date: June 17, 2004Applicant: Texas Christian UniversityInventors: Jean-Luc Montchamp, Sylvine Deprele
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Patent number: 6716984Abstract: The invention relates to the combinatorial approaches to the preparation of novel polymer-supported heteroatom bidentate (PN, PO, PS) ligand libraries and the corresponding free compounds after cleavage from the supports. These compounds are useful as novel ligands in the preparation of metal-containing catalysts.Type: GrantFiled: April 11, 2001Date of Patent: April 6, 2004Assignee: E. I. du Pont de Nemours and CompanyInventor: George Y. Li
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Publication number: 20040043967Abstract: Provided is a novel method of making bisphosphonic acids, e.g. risedronic acid, including the step of combining a carboxylic acid, phoshorous acid, and a halophosphorous compound in the presence of a diluent that is an aromatic hydrocarbon or a silicone fluid. When the diluent is an aromatic hydrocarbon, a inert support or ortho-phosphoric acid codiluent is advantageously included.Type: ApplicationFiled: May 19, 2003Publication date: March 4, 2004Inventors: Rami Lidor-Hadas, Zvi Harel, Revital Lifshitz-Liron, Eti Kovalevski-Ishai
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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: 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
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Publication number: 20030220498Abstract: A process for the production of compounds Ar—R1 by means of a cross-coupling reaction of an organometallic reagent R1—M with an aromatic or heteroaromatic substrate Ar—X catalyzed by one or several iron salts or iron complexes as catalysts or pre-catalysts, present homogeneously or heterogeneously in the reaction mixture. This new invention exhibits substantial advantages over established cross coupling methodology using palladium- or nickel complexes as the catalysts. Most notable aspects are the fact that (i) expensive and/or toxic nobel metal catalysts are replaced by cheap, stable, commercially available and toxicologically benign iron salts or iron complexes as the catalysts or pre-catalysts, (ii) commercially attractive aryl chlorides as well as various aryl sulfonates can be used as starting materials, (iii) the reaction can be performed under “ligand-free” conditons, and (iv) the reaction times are usually very short.Type: ApplicationFiled: May 10, 2002Publication date: November 27, 2003Inventors: Alois Furstner, Andreas Leitner, Maria Mendez
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Publication number: 20030166612Abstract: Novel alkenylphosphonic acid esters of the following general formula (I):Type: ApplicationFiled: December 4, 2002Publication date: September 4, 2003Inventors: Li-Biao Han, ChangQiu Zhao, Masato Tanaka