Phosphorus Attached Directly To The Five-membered Hetero Ring By Nonionic Bonding Patents (Class 548/412)
  • Patent number: 8828974
    Abstract: 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: Grant
    Filed: April 24, 2012
    Date of Patent: September 9, 2014
    Assignee: Aventis Pharmaceuticals Inc.
    Inventors: Yong Mi Choi-Sledeski, Julian Levell, Gregory Bernard Poli, Mark Czekaj, Alan John Collis, Roy Vaz
  • Publication number: 20140199600
    Abstract: 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: Application
    Filed: March 18, 2014
    Publication date: July 17, 2014
    Applicant: FUJIFILM CORPORATION
    Inventors: Toshihiko YAWATA, Ikuo KINOSHITA
  • Patent number: 8697902
    Abstract: 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: Grant
    Filed: June 5, 2009
    Date of Patent: April 15, 2014
    Assignee: Rhodia Operations
    Inventor: Sergio Mastroianni
  • Patent number: 8524628
    Abstract: 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: Grant
    Filed: July 3, 2004
    Date of Patent: September 3, 2013
    Assignee: 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
  • Patent number: 8470870
    Abstract: 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: Grant
    Filed: March 27, 2009
    Date of Patent: June 25, 2013
    Assignee: Idenix Pharmaceuticals, Inc.
    Inventors: Adel M. Moussa, Mike H. O'Neill, Xiaohong Sheng
  • Publication number: 20130126792
    Abstract: 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: Application
    Filed: July 12, 2011
    Publication date: May 23, 2013
    Applicant: Merck Patent GmbH
    Inventors: Irina Martynova, Adam W. Franz, Christof Pflumm, Amir Hossain Parham, Arne Buesing, Rémi Manouk Anémian, Anja Gerhard
  • Patent number: 8334317
    Abstract: 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: Grant
    Filed: October 15, 2008
    Date of Patent: December 18, 2012
    Assignee: 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
  • Publication number: 20120197025
    Abstract: 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: Application
    Filed: August 26, 2010
    Publication date: August 2, 2012
    Applicant: Evonik Oxeno GmbH
    Inventors: Andrea Christiansen, Robert Franke, Dirk Fridag, Dieter Hess, Burkard Kreidler, Dieter Vogt, Laura Bini, Michele Janssen, Bart Hamers
  • Patent number: 8212056
    Abstract: 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: Grant
    Filed: June 30, 2008
    Date of Patent: July 3, 2012
    Assignee: The Hong Kong Polytechnic University
    Inventors: Fuk Yee Kwong, Chau Ming So
  • Patent number: 8183231
    Abstract: 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: Grant
    Filed: October 24, 2006
    Date of Patent: May 22, 2012
    Assignee: Aventis Pharmaceuticals Inc.
    Inventors: Yong Mi Choi-Sledeski, Julian Levell, Gregory Bernard Poli, Mark Czekaj, Alan John Collis, Roy Vaz
  • Patent number: 8110709
    Abstract: 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: Grant
    Filed: October 22, 2004
    Date of Patent: February 7, 2012
    Assignee: BASF SE
    Inventors: Rainer Papp, Wolfgang Ahlers, Thomas Mackewitz, Rocco Paciello, Martin Volland
  • Publication number: 20110070194
    Abstract: 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: Application
    Filed: September 20, 2010
    Publication date: March 24, 2011
    Applicant: Gilead Sciences, Inc.
    Inventors: Aesop Cho, Choung U. Kim, Samuel E. Metobo, Adrian S. Ray, Jie Xu
  • Publication number: 20110057184
    Abstract: 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: Application
    Filed: April 30, 2009
    Publication date: March 10, 2011
    Applicant: NIPPON STEEL CHEMICAL CO., LTD.
    Inventors: Takahiro Kai, Masaki Komori, Toshihiro Yamamoto
  • Publication number: 20110039803
    Abstract: 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: Application
    Filed: March 27, 2009
    Publication date: February 17, 2011
    Inventors: Adel M. Moussa, Mike H. O'Neill, Xiaohong Sheng
  • Patent number: 7834215
    Abstract: 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: Grant
    Filed: March 2, 2006
    Date of Patent: November 16, 2010
    Assignee: Evonik Degussa GmbH
    Inventors: Jens Holz, Armin Boerner, Odalys Esperanza Zayas Vargas, Juan Jose Almena Perea, Axel Monsees, Renat Kadyrov, Thomas Riermeier
  • Publication number: 20100179324
    Abstract: 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: Application
    Filed: January 11, 2010
    Publication date: July 15, 2010
    Applicants: Microbial Chemistry Research Foundation, NIPPON KAYAKU KABUSHIKI KAISHA
    Inventors: Tetsuo AKIYAMA, Toru Masuda, Masatoshi Abe
  • Publication number: 20100099875
    Abstract: 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: Application
    Filed: June 20, 2006
    Publication date: April 22, 2010
    Applicants: PHOSPHOENIX SARL, NATIONAL INSTITUTE OF CHEMISTRY
    Inventors: Michel Stephan, Barbara Mohar
  • Publication number: 20100024133
    Abstract: Tris(heterocyclyl)-metal complexes and the use thereof as bleach catalysts are described.
    Type: Application
    Filed: October 12, 2009
    Publication date: February 4, 2010
    Applicant: Henkel AG & Co. KGaA
    Inventors: Andre Hätzelt, Anette Nordskog, Stefan Leopold, Peter Schmiedel, Wolfgang von Rybinski, Jörg Sundermeyer, Jan Döring
  • Publication number: 20090326243
    Abstract: 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: Application
    Filed: June 30, 2008
    Publication date: December 31, 2009
    Applicant: The Hong Kong Polytechnic University
    Inventors: Fuk Yee Kwong, Chau Ming So
  • Patent number: 7625939
    Abstract: 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: Grant
    Filed: May 14, 2008
    Date of Patent: December 1, 2009
    Assignee: Probiodrug AG
    Inventors: Ulrich Heiser, Andre J. Niestroj, Ulf-Torsten Gaertner, Hans-Ulrich Demuth
  • Publication number: 20090281330
    Abstract: 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: Application
    Filed: July 6, 2007
    Publication date: November 12, 2009
    Inventors: Paul Tordo, Jean-Pierre Bernard Finet, Florence Nathalie Laurence Chalier, Olivier Ouari, Micael Hardy
  • Patent number: 7589215
    Abstract: 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: Grant
    Filed: December 12, 2006
    Date of Patent: September 15, 2009
    Assignee: Degussa AG
    Inventors: Armin Boerner, Jens Holz, Axel Monsees, Thomas Riermeier, Renat Kadyrov, Carsten A. Schneider, Uwe Dingerdissen, Karlheinz Drauz
  • Patent number: 7589081
    Abstract: 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: Grant
    Filed: May 3, 2004
    Date of Patent: September 15, 2009
    Assignee: DEGUSSA GmbH
    Inventors: Alexander Zapf, Mark Sundermeier, Ralf Jackstell, Matthias Beller, Thomas Riermeier, Axel Monsees, Uwe Dingerdissen
  • Publication number: 20090227801
    Abstract: 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: Application
    Filed: October 10, 2005
    Publication date: September 10, 2009
    Applicant: BASF AKTIENGESELLSCHAFT
    Inventors: Wolfgang Ahlers, Martina Egen, Martin Volland, Christoph Jakel, Frank Hettche, Rocco Paciello
  • Publication number: 20090169475
    Abstract: Methods of imaging tissue of a mammal which expresses chymase include administering to the mammal an effective amount of a radiolabeled chymase inhibitor.
    Type: Application
    Filed: December 18, 2008
    Publication date: July 2, 2009
    Inventors: John W. Babich, William C. Eckelman, John Joyal, Craig Zimmerman
  • Publication number: 20090163444
    Abstract: 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: Application
    Filed: November 21, 2008
    Publication date: June 25, 2009
    Inventors: Richard Storer, Cyril Dousson, Francois-Rene Alexandre, Arlene Roland
  • Patent number: 7550406
    Abstract: 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: Grant
    Filed: July 3, 2004
    Date of Patent: June 23, 2009
    Assignee: 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
  • Patent number: 7531657
    Abstract: 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: Grant
    Filed: December 16, 2002
    Date of Patent: May 12, 2009
    Assignee: Nippon Kayaku Kabushiki Kaisha
    Inventors: Masashi Nagai, Hiroko Yamazaki, Keiichirou Yamamoto, Masatoshi Abe
  • Patent number: 7511154
    Abstract: 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: Grant
    Filed: July 26, 2007
    Date of Patent: March 31, 2009
    Assignee: Basilea Pharmaceuticals AG
    Inventor: Mark Rogers-Evans
  • Publication number: 20080306264
    Abstract: 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: Application
    Filed: April 14, 2005
    Publication date: December 11, 2008
    Applicant: Degussa AG
    Inventors: Renat Kadyrov, Juan Jose Almena Perea, Axel Monsees, Thomas Riermeier, Ilias Z. Ilaldinov
  • Publication number: 20080269492
    Abstract: 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: Application
    Filed: October 12, 2006
    Publication date: October 30, 2008
    Applicant: BRIDGESTONE CORPORATION
    Inventors: Masashi Otsuki, Hiroshi Kanno
  • Publication number: 20080200695
    Abstract: 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: Application
    Filed: March 2, 2006
    Publication date: August 21, 2008
    Applicant: DEGUSSA GmbH
    Inventors: Jens Holz, Armin Boerner, Odalys Esperanza Zayas Vargas, Juan Jose Almena Perea, Axel Monsees, Renat Kadyrov, Thomas Riermeier
  • Patent number: 7348318
    Abstract: 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: Grant
    Filed: March 24, 2003
    Date of Patent: March 25, 2008
    Assignees: Nippon Kayaku Kabushiki Kaisha, Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai
    Inventors: Masatoshi Abe, Masashi Nagai, Keiichirou Yamamoto, Chihiro Nishimura
  • Publication number: 20080009636
    Abstract: 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: Application
    Filed: October 24, 2006
    Publication date: January 10, 2008
    Inventors: Paul Tordo, Jean-Pierre Bernard Finet, Florence Nathalie Laurence Chalier, Olivier Ouari, Micael Hardy
  • Patent number: 7307037
    Abstract: 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: Grant
    Filed: March 3, 2003
    Date of Patent: December 11, 2007
    Assignee: Chemi S.p.A.
    Inventors: Francesco Sannicolo′, Oreste Piccolo, Tiziana Benincori, Mara Sada, Alessandra Verrazzani, Simona Tollis, Elio Ullucci, Lorenzo De Ferra, Simona Rizzo
  • Patent number: 7247640
    Abstract: 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: Grant
    Filed: July 22, 2005
    Date of Patent: July 24, 2007
    Assignees: Nippon Kayaku Kabushiki Kaisha, Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai
    Inventors: Takumi Yamashita, Chihiro Nishimura, Tetsushi Saino, Yasuhiko Muraoka, Tomio Takeuchi
  • Patent number: 7173138
    Abstract: 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: Grant
    Filed: March 28, 2002
    Date of Patent: February 6, 2007
    Assignee: BASF Aktiengesellschaft
    Inventors: Wolfgang Ahlers, Rocco Paciello, Dieter Vogt, Peter Hofmann
  • Patent number: 7105556
    Abstract: 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: Grant
    Filed: May 22, 2002
    Date of Patent: September 12, 2006
    Assignee: Bristol-Myers Squibb Company
    Inventors: Peter T. Cheng, Yoon Jeon, Wei Wang
  • Patent number: 7094907
    Abstract: 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 s
    Type: Grant
    Filed: October 2, 2002
    Date of Patent: August 22, 2006
    Assignee: Solvias AG
    Inventor: Ulrich Berens
  • Patent number: 7081536
    Abstract: 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 of
    Type: Grant
    Filed: August 1, 2002
    Date of Patent: July 25, 2006
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: Nicole End, Catherine Stoessel, Ulrich Berens, Pier Giorgio Cozzi
  • Patent number: 6902586
    Abstract: 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: Grant
    Filed: July 2, 2002
    Date of Patent: June 7, 2005
    Assignee: L'Oreal
    Inventors: Rui Pereira, Richard Martin
  • Patent number: 6900238
    Abstract: 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: Grant
    Filed: December 9, 1996
    Date of Patent: May 31, 2005
    Assignee: The Scripps Research Institute
    Inventors: Chi-Huey Wong, Deborah H. Slee, Karen Laslo
  • Patent number: 6828442
    Abstract: 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: Grant
    Filed: February 14, 2003
    Date of Patent: December 7, 2004
    Assignee: Basilea Pharmaceutica AG
    Inventor: Mark Rogers-Evans
  • Publication number: 20040138495
    Abstract: 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: Application
    Filed: December 17, 2003
    Publication date: July 15, 2004
    Inventors: Klaus Haaf, Marcel Patek
  • Publication number: 20040116702
    Abstract: 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: Application
    Filed: October 14, 2003
    Publication date: June 17, 2004
    Inventors: Ralf Noe, Andreas Henne, Matthias Maase
  • Publication number: 20040116713
    Abstract: N-Phenylpyrrolebisphosphines of the formula I 1
    Type: Application
    Filed: January 20, 2004
    Publication date: June 17, 2004
    Inventors: Matthias Beller, Ralf Jackstell, Holger Klein, Detlef Heller, Hans-Joachim Drexler, Klaus-Diether Wiese, Dirk Rottger
  • Publication number: 20040077605
    Abstract: 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: Application
    Filed: December 18, 2002
    Publication date: April 22, 2004
    Inventors: 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
  • Publication number: 20040039189
    Abstract: 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: Application
    Filed: July 30, 2003
    Publication date: February 26, 2004
    Inventors: Ramon Guimil, Matthias Scheffler
  • Publication number: 20030232991
    Abstract: 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: Application
    Filed: April 10, 2003
    Publication date: December 18, 2003
    Applicant: The Penn State Research Foundation
    Inventor: Xumu Zhang
  • Publication number: 20030225284
    Abstract: 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: Application
    Filed: April 11, 2002
    Publication date: December 4, 2003
    Inventors: Quanlai Song, Bruce Ross