The Hetero Ring Is Five-membered Patents (Class 549/6)
  • Publication number: 20140311575
    Abstract: The present invention relates to modified surfaces. The surfaces comprise an inorganic material on which a phosphinic acid derivative is adsorbed. The phosphinic acid thus turns out to be a new anchoring group useful for surface derivatisation. The invention has many applications for photoelectric conversion devices, batteries, capacitors, electrochromic displays, chemical sensors, biological sensors, light emitting diodes, electrodes, semiconductors, separation membranes, selective adsorbents, adsorbents for HPLC, catalysts, implants, nanoparticles, antiadhesives, and anticorrosion coatings, for example.
    Type: Application
    Filed: June 30, 2014
    Publication date: October 23, 2014
    Inventors: Shaik Mohammad Zakeeruddin, Peter Pechy, Michael Graetzel
  • Publication number: 20140290748
    Abstract: The present invention relates to an organic colorant corresponding to one of the following structures (I) or (II): eD-pi-conjugated chromophore-L-A??(I) A-L-pi-conjugated chromophore-eD??(II) in which eD represents an electron donor segment; L represents a covalent bond or a spacer segment; A represents an electron attractor segment able to form a covalent bond with a semi-conductor; the pi-conjugated chromophore comprising at least two aromatic rings, at least one of which is a thiophene, selenophene or furan type ring. The present invention relates to the use thereof as photosensitizer in a photovoltaic device and said photovoltaic device.
    Type: Application
    Filed: November 12, 2012
    Publication date: October 2, 2014
    Applicant: COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES
    Inventors: Renaud Demadrille, Yann Kervella
  • Patent number: 8765722
    Abstract: Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.
    Type: Grant
    Filed: June 26, 2013
    Date of Patent: July 1, 2014
    Assignee: Gilead Sciences, Inc.
    Inventors: Aesop Cho, Lee S. Chong, Michael O'Neil Hanrahan Clarke, Edward Doerffler, Choung U. Kim, Qi Liu, William J. Watkins, Jennifer R. Zhang
  • Patent number: 8754066
    Abstract: The present invention relates to novel phenoxy derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Grant
    Filed: February 20, 2013
    Date of Patent: June 17, 2014
    Assignee: Allergan, Inc.
    Inventors: Wenkui K. Fang, Liming Wang, Ken Chow, Evelyn G. Corpuz, Wha-Bin Im
  • Publication number: 20140161839
    Abstract: The present invention relates to a compound of the following general formula (I): R1—NH—CH(R2)—P(?O)(OR3)—CH2—C(R4)(R5)—CONH—CH(R6)—COOR7 (I) or a pharmaceutically acceptable salt of the latter, an isomer or a mixture of isomers in any proportions, especially a mixture of enantiomers, and in particular a racemic mixture, for which R1 represents a —C(?O)—O—C(R8)(R9)—OC(?O)—R10 group; R2 represents an optionally substituted hydrocarbon-based chain, an aryl or heteroaryl group or a methylene group substituted by a heterocycle; R3 represents a hydrogen atom or a —C(R12)(R13)—OC(?O)—R14 group; R4 and R5 form, together with the carbon that bears them, a saturated hydrocarbon-based ring or an optionally substituted piperidine ring or R4 represents a hydrogen atom and R5 represents a phenyl or a benzyl that is optionally substituted, a heteroaromatic ring or a methylene group substituted by a heterocycle; R6 represents an optionally substituted hydrocarbon-based chain or a phenyl or a benzyl that is optionally substi
    Type: Application
    Filed: February 18, 2014
    Publication date: June 12, 2014
    Applicant: PHARMALEADS
    Inventors: Bernard Roques, Herve Poras, Marie-Claude Fournie-Zaluski
  • Publication number: 20140135293
    Abstract: The present invention relates to allene derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: November 7, 2013
    Publication date: May 15, 2014
    Applicant: ALLERGAN, INC.
    Inventors: WENKUI K. FANG, Evelyn G. Corpuz, Ken Chow, WhaBin Im
  • Publication number: 20140107075
    Abstract: The present invention relates to novel amine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: February 21, 2013
    Publication date: April 17, 2014
    Applicant: ALLERGAN, INC.
    Inventors: TODD M. HEIDELBAUGH, PHONG X. NGUYEN
  • Publication number: 20140100194
    Abstract: The invention is directed to TRPM8 antagonists of Formula (I). More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating TRPM8-mediated disorders. Pharmaceutical and veterinary compositions and methods of treating pain and various other disease states or conditions using compounds of the invention are also described.
    Type: Application
    Filed: December 5, 2013
    Publication date: April 10, 2014
    Applicant: Janssen Pharmaceutica, NV
    Inventors: Raymond W Colburn, Scott L. Dax, Christopher M. Flores, Jay M. Matthews
  • Patent number: 8664204
    Abstract: Phosphoramidate alkylator prodrugs can be used to treat cancer when administered alone or in combination with one or more anti-neoplastic agents.
    Type: Grant
    Filed: July 12, 2013
    Date of Patent: March 4, 2014
    Assignee: Threshold Pharmaceuticals, Inc.
    Inventors: Mark Matteucci, Jian-Xin Duan, Hailong Jiao
  • Publication number: 20140012016
    Abstract: Provided is an efficient technology for synthesizing diamino acids (diamino acid derivatives). Disclosed is a manufacturing method for diamino acid derivatives wherein the fluorenyl groups of the diamino acid derivative starting materials represented by General Formula [II] or [IV] are removed.
    Type: Application
    Filed: September 11, 2013
    Publication date: January 9, 2014
    Applicant: Japan Science and Technology Agency
    Inventors: Shu KOBAYASHI, Yasuhiro YAMASHITA, Kazutaka SEKI
  • Publication number: 20130302280
    Abstract: Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.
    Type: Application
    Filed: June 26, 2013
    Publication date: November 14, 2013
    Inventors: Aesop Cho, Lee S. Chong, Michael O'Neil Hanrahan Clarke, Edward Doerffler, Choung U. Kim, Qi Liu, William J. Watkins, Jennifer R. Zhang
  • Publication number: 20130274484
    Abstract: An aromatic compound bearing at least a phosphonate or phosphinate group on the aromatic ring is described. Further described, is the process by which the aromatic compound is prepared, reacted with a reagent of formula (I) or (II) constituted of a diene backbone and bearing a phosphonate or phosphinate group on one of the double bonds, in the presence of a Lewis acid.
    Type: Application
    Filed: December 24, 2010
    Publication date: October 17, 2013
    Inventors: Floryan De Campo, Tao Zhang, Changkai Zhou
  • Patent number: 8558011
    Abstract: The invention is directed to TRPM8 antagonists of Formula (I). More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating TRPM8-mediated disorders. Pharmaceutical and veterinary compositions and methods of treating pain and various other disease states or conditions using compounds of the invention are also described.
    Type: Grant
    Filed: August 31, 2010
    Date of Patent: October 15, 2013
    Assignee: Janssen Pharmaceutica, NV
    Inventors: Raymond W Colburn, Scott L Dax, Christopher Flores, Jay M Matthews
  • Patent number: 8541397
    Abstract: The present invention relates to novel alkyne and alkene derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Grant
    Filed: February 5, 2013
    Date of Patent: September 24, 2013
    Assignee: Allergan, Inc.
    Inventors: Santosh C. Sinha, Smita Bhat, Evelyn Corpuz, Ken Chow, Wenkui K. Fang, Wha-Bin Im
  • Publication number: 20130217651
    Abstract: The present invention relates to novel phenoxy derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: February 20, 2013
    Publication date: August 22, 2013
    Applicant: ALLERGAN, INC.
    Inventor: ALLERGAN, INC.
  • Patent number: 8507464
    Abstract: Phosphoramidate alkylator prodrugs can be used to treat cancer when administered alone or in combination with one or more anti-neoplastic agents.
    Type: Grant
    Filed: June 17, 2011
    Date of Patent: August 13, 2013
    Assignee: Threshold Pharmaceuticals, Inc.
    Inventors: Mark Matteucci, Jian-Xin Duan, Hailong Jiao, Jacob Kaizerman
  • Patent number: 8501714
    Abstract: Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.
    Type: Grant
    Filed: September 7, 2010
    Date of Patent: August 6, 2013
    Assignee: Gilead Sciences, Inc.
    Inventors: Aesop Cho, Lee S. Chong, Michael O'Neil Hanrahan Clarke, Edward Doerffler, Choung U. Kim, Qi Liu, William J. Watkins, Jennifer R. Zhang
  • Publication number: 20130157982
    Abstract: The present invention relates to novel amine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: February 11, 2013
    Publication date: June 20, 2013
    Applicant: ALLERGAN, INC.
    Inventor: ALLERGAN, INC.
  • Publication number: 20130150331
    Abstract: The present invention relates to novel alkyne and alkene derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: February 5, 2013
    Publication date: June 13, 2013
    Applicant: ALLERGAN, INC.
    Inventor: ALLERGAN, INC.
  • Patent number: 8450501
    Abstract: Compounds of the formula (I), in the form of mixtures comprising predominantly one diastereomer or in the form of pure diastereomers, Z1-Q-P*R0R1 (I) in which Z1 is a C-bonded, secondary phosphine group —P(R)2; in which R is in each case independently hydrocarbon radicals or heterohydrocarbon radicals, or Z1 is the —P*R0R1 group; Q is a bivalent, achiral, aromatic base skeleton, a bivalent, achiral ferrocene base skeleton, an optionally substituted bivalent cycloalkane or heterocycloalkane skeleton, or a C1-C4-alkylene skeleton.
    Type: Grant
    Filed: November 14, 2008
    Date of Patent: May 28, 2013
    Assignee: Solvias AG
    Inventors: Benoît Pugin, Matthias Lotz, Heidi Landert, Adrian Wyss, Raphael Aardoom, Björn Gschwend, Andreas Pfaltz, Felix Spindler
  • 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: 8415488
    Abstract: Compounds of the formula I, in the form of mixtures comprising predominantly one enantiomer or in the form of pure enantiomers, secondary phosphine-Q-P*(?O)HR1 (I) in which secondary phosphine is a C-bonded, secondary phosphine group —P(R)2; in which R is in each case independently hydrocarbon radicals or heterohydrocarbon radicals; Q is a bivalent, achiral, aromatic base skeleton, a bivalent, achiral ferrocene base skeleton, an optionally substituted bivalent cycloalkane or heterocycloalkane skeleton, or a C1-C4-alkylene skeleton, and in which base skeletons a secondary phosphine group is bonded directly to a carbon atom, or, in the case of cyclic base skeletons, directly to a carbon atom or via a C1-C4-alkylene group, and in which base skeletons a P-chiral group —P*(O)HR1 is bonded to a carbon atom such that the phosphorus atoms are linked via 1 to 7 atoms of a carbon chain optionally interrupted by heteroatoms from the group of O, S, N, Fe or Si; P* is a chiral phosphorus atom; and R1 is a hydrocarbon radi
    Type: Grant
    Filed: November 14, 2008
    Date of Patent: April 9, 2013
    Assignee: Solvias AG
    Inventors: Benoît Pugin, Heidi Landert, Björn Gschwend, Andreas Pfaltz, Felix Spindler
  • Patent number: 8404663
    Abstract: The present invention relates to novel alkyne and alkene derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Grant
    Filed: November 28, 2011
    Date of Patent: March 26, 2013
    Assignee: Allergan, Inc.
    Inventors: Santosh C. Sinha, Smita S. Bhat, Evelyn G. Corpuz, Ken Chow, Wenkui K. Fang, Wha-Bin Im
  • Patent number: 8378122
    Abstract: The present invention is a process for the preparation of chymase modulators, useful in the treatment of inflammatory and serine protease mediated disorders.
    Type: Grant
    Filed: August 9, 2012
    Date of Patent: February 19, 2013
    Assignee: Janssen Pharmaceutica NV.
    Inventors: Luigi Anzalone, Penina Feibush, Ilias Konstantinos Dorziotis, Frank J. Villani
  • Publication number: 20120309986
    Abstract: The present invention is a process for the preparation of chymase modulators, useful in the treatment of inflammatory and serine protease mediated disorders.
    Type: Application
    Filed: August 9, 2012
    Publication date: December 6, 2012
    Inventors: Luigi Anzalone, Penina Feibush, IIias Konstantinos Dorziotis, Xun Li, Frank J. Villani
  • Publication number: 20120283222
    Abstract: Compounds represented by formula (I): wherein each symbol is as defined in the description, and pharmaceutically acceptable salts thereof are useful as hyperglycemic inhibitors having a serine protease inhibitory action and as prophylactic or therapeutic drugs for diabetes.
    Type: Application
    Filed: May 31, 2012
    Publication date: November 8, 2012
    Applicant: Ajinomoto Co., Inc.
    Inventors: Atsushi KONISHI, Munetaka Tokumasu, Tamotsu Suzuki, Takahiro Koshiba, Koji Ohsumi, Osamu Ikehara, Yuko Kodama
  • Publication number: 20120259130
    Abstract: The present invention is directed to an improved process for synthesizing phosphonic and phosphinic acid chymase inhibitor compounds.
    Type: Application
    Filed: June 19, 2012
    Publication date: October 11, 2012
    Inventors: Luigi Anzalone, Daniel J. Pippel, Neelakandha S. Mani, Penina Feibush, IIias K. Dorziotis, Stefan Horns, Frank J. Villani, JR.
  • Publication number: 20120184510
    Abstract: The invention is directed to TRPM8 antagonists of Formula (I). More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating TRPM8-mediated disorders. Pharmaceutical and veterinary compositions and methods of treating pain and various other disease states or conditions using compounds of the invention are also described.
    Type: Application
    Filed: January 14, 2011
    Publication date: July 19, 2012
    Inventors: Raymond W. Colburn, Scott L. Dax, Christopher Flores, Jay Matthews, Ning Qin, Laura Reany, Christopher Teleha, Mark A. Youngman
  • Publication number: 20120156166
    Abstract: Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.
    Type: Application
    Filed: September 7, 2010
    Publication date: June 21, 2012
    Applicant: Gilead Sciences, Inc.
    Inventors: Aesop Cho, Lee S. Chong, Michael O' Neil Hanrahan Clarke, Edward Doerffler, Choung U. Kim, Qi Liu, William J. Watkins, Jennifer R. Zhang
  • Patent number: 8197722
    Abstract: Compositions capable of simultaneous two-photon absorption and higher order absorptivities are provided. Compounds having a donor-pi-donor or acceptor-pi-acceptor structure are of particular interest, where the donor is an electron donating group, acceptor is an electron accepting group, and pi is a pi bridge linking the donor and/or acceptor groups. The pi bridge may additionally be substituted with electron donating or withdrawing groups to alter the absorptive wavelength of the structure. Also disclosed are methods of generating an excited state of such compounds through optical stimulation with light using simultaneous absorption of photons of energies individually insufficient to achieve an excited state of the compound, but capable of doing so upon simultaneous absorption of two or more such photons. Applications employing such methods are also provided, including controlled polymerization achieved through focusing of the light source(s) used.
    Type: Grant
    Filed: July 30, 2001
    Date of Patent: June 12, 2012
    Assignee: The California Institute of Technology
    Inventors: Seth Marder, Joseph Perry
  • Publication number: 20120142805
    Abstract: The invention pertains to an oligomer or polymer substituted by one or more bisacylphosphine oxide moieties, characterized in that said bisacylphosphine oxide moiety is linked via the phosphorous atom, optionally via a spacer group, to the oligomer or polymer backbone; as well as to specifically functionalized bisacylphosphine oxides, suitable to prepare said polymers or oligomers.
    Type: Application
    Filed: June 29, 2010
    Publication date: June 7, 2012
    Applicant: BASF SE
    Inventors: Hansjorg Grutzmacher, Timo Ott, Kurt Dietliker
  • Publication number: 20120142640
    Abstract: The present invention relates to novel alkyne and alkene derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: November 28, 2011
    Publication date: June 7, 2012
    Applicant: ALLERGAN, INC.
    Inventors: Santosh C. Sinha, Smita S. Bhat, Evelyn G. Corpuz, Ken Chow, Wenkui K. Fang, Wha-Bin Im
  • Patent number: 8193372
    Abstract: Provided herein are phosphothiophene and phosphothiazole compounds, for example, of any of Formulae I, IA, IIA, IIIA, IVA, VA, VIA, VIIA, IB, IIB, IIIB, IVB, VB, VIB and VIIB disclosed herein, 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 infected with HCV.
    Type: Grant
    Filed: March 3, 2010
    Date of Patent: June 5, 2012
    Assignee: Idenix Pharmaceuticals, Inc.
    Inventors: Cyril Dousson, Claire Pierra, Jean-Francois Griffon, Frederic Leroy, Jean-Laurent Paparin, David Dukhan, Dominique Surleraux
  • Publication number: 20120053347
    Abstract: The invention is directed to TRPM8 antagonists of Formula (I). More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating TRPM8-mediated disorders. Pharmaceutical and veterinary compositions and methods of treating pain and various other disease states or conditions using compounds of the invention are also described.
    Type: Application
    Filed: August 31, 2010
    Publication date: March 1, 2012
    Inventors: Raymond W. Colburn, Scott L. Dax, Christopher Flores, Jay Matthews
  • Patent number: 8105504
    Abstract: Organic materials which possess outstanding stability to oxidative, thermal or light-induced degradation comprise as stabilizers at least one compound of the formula (I) wherein the general symbols are as defined in claim 1. The compounds of formula I are especially useful as stabilizers for protecting polymers and lubricants against oxidative, thermal or light-induced degradation and as scavengers for oxidized developer in color photographic material.
    Type: Grant
    Filed: August 22, 2005
    Date of Patent: January 31, 2012
    Assignee: BASF SE
    Inventors: Michèle Gerster, Peter Nesvadba
  • Patent number: 8039496
    Abstract: Disclosed herein is a compound of the formula. Therapeutic methods, compositions, and medicaments for the treatment of glaucoma or ocular hypertension related thereto are also disclosed.
    Type: Grant
    Filed: January 22, 2008
    Date of Patent: October 18, 2011
    Assignee: Allergan, Inc.
    Inventors: David W. Old, Vinh X. Ngo
  • Publication number: 20110251159
    Abstract: Phosphoramidate alkylator prodrugs can be used to treat cancer when administered alone or in combination with one or more anti-neoplastic agents.
    Type: Application
    Filed: June 17, 2011
    Publication date: October 13, 2011
    Applicant: Threshold Pharmaceuticals, Inc.
    Inventors: Mark Matteucci, Jian-Xin Duan, Hailong Jiao, Jacob Kaizerman
  • Patent number: 8030438
    Abstract: A thiophene compound having a phosphate group, for example, one represented by the formula [1]. The compound has high resistance to heat and oxidation and can be improved in solubility or dispersibility in various solvents. (In the formula, R1 and R2 each independently represents, e.g., hydrogen, halogeno, cyano, or phenyl optionally substituted by W; and R3 to R6 each independently represents —OR7, SR8, or —NR92, provided that R7 to R9 each independently represents hydrogen, C1-10 alkyl, or phenyl optionally substituted by W and W represents halogeno, cyano, nitro, hydroxyl, mercapto, amino, formyl, carboxy, C1-10 alkyl, etc.
    Type: Grant
    Filed: May 16, 2006
    Date of Patent: October 4, 2011
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Nobuyuki Kakiuchi, Hitoshi Furusho, Naoki Otani, Tohru Minami, Tatsuo Okauchi
  • Patent number: 8003625
    Abstract: Phosphoramidate alkylator prodrugs can be used to treat cancer when administered alone or in combination with one or more anti-neoplastic agents.
    Type: Grant
    Filed: June 29, 2006
    Date of Patent: August 23, 2011
    Assignee: Threshold Pharmaceuticals, Inc.
    Inventors: Mark Matteucci, Jian-Xin Duan, Hailong Jiao, Jacob Kaizerman
  • Patent number: 7981874
    Abstract: The present invention relates to a novel class of phosphorus derivatives. The phosphorus compounds can be used to treat cancer. The phosphorus compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.
    Type: Grant
    Filed: July 16, 2007
    Date of Patent: July 19, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Joshua Close, Jonathan Grimm, Richard W. Heidebrecht, Jr., Solomon Kattar, Thomas A. Miller, Karin M. Otte, Scott Peterson, Phieng Siliphaivanh, Paul J. Tempest, Kevin J. Wilson, David J. Witter
  • Publication number: 20110124601
    Abstract: The present invention relates to a compound of the following general formula (I): R1—NH—CH(R2)—P(?O)(OR3)—CH2—C(R4)(R5)—CONH—CH(R6)—COOR7 (I) or a pharmaceutically acceptable salt of the latter, an isomer or a mixture of isomers in any proportions, especially a mixture of enantiomers, and in particular a racemic mixture, for which R1 represents a —C(?O)—O—C(R8)(R9)—OC(?O)—R10 group; R2 represents an optionally substituted hydrocarbon-based chain, an aryl or heteroaryl group or a methylene group substituted by a heterocycle; R3 represents a hydrogen atom or a —C(R12)(R13)—OC(?O)—R14 group; R4 and R5 form, together with the carbon that bears them, a saturated hydrocarbon-based ring or an optionally substituted piperidine ring or R4 represents a hydrogen atom and R5 represents a phenyl or a benzyl that is optionally substituted, a heteroaromatic ring or a methylene group substituted by a heterocycle; R6 represents an optionally substituted hydrocarbon-based chain or a phenyl or a benzyl that is optionally substi
    Type: Application
    Filed: July 22, 2009
    Publication date: May 26, 2011
    Inventors: Bernard Roques, Hervé Poras, Marie-Claude Fournie-Zaluski
  • Publication number: 20110118482
    Abstract: Compounds of the formula (I), in the form of mixtures comprising predominantly one diastereomer or in the form of pure diastereomers, Z1-Q-P*R0R1 (I) in which Z1 is a C-bonded, secondary phosphine group —P(R)2; in which R is in each case independently hydrocarbon radicals or heterohydrocarbon radicals, or Z1 is the —P*R0R1 group; Q is a bivalent, achiral, aromatic base skeleton, a bivalent, achiral ferrocene base skeleton, an optionally substituted bivalent cycloalkane or heterocycloalkane skeleton, or a C1-C4-alkylene skeleton, and in which base skeletons a secondary phosphine group Z1 is bonded directly to a carbon atom, or, in the case of cyclic base skeletons, directly to a carbon atom or via a C1-C4-alkylene group, and in which base skeletons a P-chiral group —P*R0R1 is bonded directly to a carbon atom, or, in the case of cyclic base skeletons, directly to a carbon atom or via a C1-C4-alkylene group to a carbon atom such that the phosphorus atoms are linked via 1 to 7 atoms of a carbon chain optionally i
    Type: Application
    Filed: November 14, 2008
    Publication date: May 19, 2011
    Inventors: Benoît Pugin, Matthias Lotz, Heidi Landert, Adrian Wyss, Raphael Aardoom, Bjõrn Gschwend, Andreas Pfaltz, Felix Spindler
  • Publication number: 20110098485
    Abstract: Compounds of the formula I, in the form of mixtures comprising predominantly one enantiomer or in the form of pure enantiomers, secondary phosphine-Q-P*(?O)HR1 (I) in which secondary phosphine is a C-bonded, secondary phosphine group —P(R)2; in which R is in each case independently hydrocarbon radicals or heterohydrocarbon radicals; Q is a bivalent, achiral, aromatic base skeleton, a bivalent, achiral ferrocene base skeleton, an optionally substituted bivalent cycloalkane or heterocycloalkane skeleton, or a C1-C4-alkylene skeleton, and in which base skeletons a secondary phosphine group is bonded directly to a carbon atom, or, in the case of cyclic base skeletons, directly to a carbon atom or via a C1-C4-alkylene group, and in which base skeletons a P-chiral group —P*(O)HR1 is bonded to a carbon atom such that the phosphorus atoms are linked via 1 to 7 atoms of a carbon chain optionally interrupted by heteroatoms from the group of O, S, N, Fe or Si; P* is a chiral phosphorus atom; and R1 is a hydrocarbon radi
    Type: Application
    Filed: November 14, 2008
    Publication date: April 28, 2011
    Inventors: Benoît Pugin, Heidi Landert, Björn Gschwend, Andreas Pfaltz, Felix Spindler
  • Publication number: 20100317625
    Abstract: This invention provides novel ?-lactamase inhibitors of the aryl- and heteroaryl-sulfonamidomethylphosphonate monoester class. The compounds inhibit three classes of ?-lactamases and synergize the antibacterial effects of ?-lactam antibiotics (e.g., imipenem and ceftazimdime) against those micro-organisms normally resistant to the ?-lactam antibiotics as a result of the presence of the ?-lactamases.
    Type: Application
    Filed: May 21, 2007
    Publication date: December 16, 2010
    Inventors: Frank Dininno, Milton L. Hammond, Kevin Dykstra, Seongkon Kim, Qiang Tan, Katherine Young, Jeffrey Donald Hermes, Stephane Raeppel, Michael Mannion, Nancy Z. Zhou, Frederic Gaudette, Arkadii Vaisburg, Jubrail Rahil, Nafsika Georgopapadakou
  • Publication number: 20100279983
    Abstract: This invention provides novel ?-lactamase inhibitors of the aryl- and heteroarylsulfonamidomethylphosphonate monoester class having nitrogen-based cations or quarternary ammonium groups. The compounds inhibit three classes of ?-lactamases and synergize the antibacterial effects of ?-lactam antibiotics (e.g., imipenem and ceftazidime) against those micro-organisms normally resistant to the ?-lactam antibiotics as a result of the presence of the ?-lactamases. Formula (I) or pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: May 21, 2007
    Publication date: November 4, 2010
    Inventors: Frank Dininno, Milton L. Hammond, Kevin Dykstra, Seongkon Kim, Qiang Tan, Katherine Young, Jeffrey Donald Hermes, Helen Chen, Stephane Raeppel, Michael Mannion, Frederic Gaudette, Arkadii Vaisburg, Jubrail Rahil, Nafsika Georgopapadakou, Nancy Z. Zhou
  • Publication number: 20100233123
    Abstract: Provided herein are phosphothiophene and phosphothiazole compounds, for example, of any of Formulae I, IA, IIA, IIIA, IVA, VA, VIA, VIIA, IB, IIB, IIIB, IVB, VB, VIIB and VIIB disclosed herein, 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 infected with HCV.
    Type: Application
    Filed: March 3, 2010
    Publication date: September 16, 2010
    Applicant: Idenix Pharmaceuticals, Inc.
    Inventors: Cyril Dousson, Claire Pierra, Jean-Francois Griffon, Frederic Leroy, Jean-Laurent Paparin, David Dukhan, Dominique Surleraux
  • Patent number: 7763739
    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: Grant
    Filed: April 14, 2005
    Date of Patent: July 27, 2010
    Assignee: Evonik Degussa, GmbH
    Inventors: Renat Kadyrov, Juan José Almena Perea, Axel Monsees, Thomas Riermeier, Ilias Ilaldinov
  • Publication number: 20100174079
    Abstract: 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: Application
    Filed: August 20, 2007
    Publication date: July 8, 2010
    Applicant: National Institute of Advanced Industrial Science Technology
    Inventors: Li-Biao Han, Qing Xu
  • Publication number: 20100145075
    Abstract: The present invention is a process for the preparation of chymase modulators, useful in the treatment of inflammatory and serine protease mediated disorders.
    Type: Application
    Filed: October 29, 2009
    Publication date: June 10, 2010
    Inventors: Luigi Anzalone, Penina Feibush, Ilias Konstantinos Dorziotis, Xun Li, Frank J. Villani
  • Publication number: 20100137254
    Abstract: Phosphoramidate alkylator prodrugs can be used to treat cancer when administered along or in combination with one or more anti-neoplastic agents.
    Type: Application
    Filed: June 29, 2006
    Publication date: June 3, 2010
    Inventors: Mark Matteucci, Jian-Xin Duan, Hailong Jiao