The Hetero Ring Is Five-membered Patents (Class 549/6)
-
Patent number: 11994799Abstract: A negative resist composition is provided comprising a base polymer and an acid generator in the form of a sulfonium salt consisting of a sulfonate anion having a maleimide group and a cation having a polymerizable double bond. The resist composition adapted for organic solvent development exhibits a high resolution and improved LWR or CDU.Type: GrantFiled: July 14, 2022Date of Patent: May 28, 2024Assignee: SHIN-ETSU CHEMICAL CO., LTD.Inventor: Jun Hatakeyama
-
Patent number: 11812659Abstract: An organic electroluminescence device of an embodiment includes a first electrode, a second electrode opposite the first electrode, and an emission layer between the first electrode and the second electrode, wherein the emission layer includes a polycyclic compound represented by Formula 1, thereby showing improved emission efficiency.Type: GrantFiled: September 22, 2020Date of Patent: November 7, 2023Assignees: Samsung Display Co., Ltd., Lapto Co., Ltd.Inventors: Seulong Kim, Eu-gene Oh, Munsoo Kim, JuWan Maeng, Kap-jong Han, Jaeweon Hur, Hyewon Choi, Kyungsik Kim, Sung-Soo Bae
-
Publication number: 20140311575Abstract: 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: ApplicationFiled: June 30, 2014Publication date: October 23, 2014Inventors: Shaik Mohammad Zakeeruddin, Peter Pechy, Michael Graetzel
-
Publication number: 20140290748Abstract: 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: ApplicationFiled: November 12, 2012Publication date: October 2, 2014Applicant: COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVESInventors: Renaud Demadrille, Yann Kervella
-
Patent number: 8765722Abstract: 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: GrantFiled: June 26, 2013Date of Patent: July 1, 2014Assignee: 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: 8754066Abstract: 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: GrantFiled: February 20, 2013Date of Patent: June 17, 2014Assignee: Allergan, Inc.Inventors: Wenkui K. Fang, Liming Wang, Ken Chow, Evelyn G. Corpuz, Wha-Bin Im
-
Publication number: 20140161839Abstract: 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 substiType: ApplicationFiled: February 18, 2014Publication date: June 12, 2014Applicant: PHARMALEADSInventors: Bernard Roques, Herve Poras, Marie-Claude Fournie-Zaluski
-
Publication number: 20140135293Abstract: 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: ApplicationFiled: November 7, 2013Publication date: May 15, 2014Applicant: ALLERGAN, INC.Inventors: WENKUI K. FANG, Evelyn G. Corpuz, Ken Chow, WhaBin Im
-
Publication number: 20140107075Abstract: 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: ApplicationFiled: February 21, 2013Publication date: April 17, 2014Applicant: ALLERGAN, INC.Inventors: TODD M. HEIDELBAUGH, PHONG X. NGUYEN
-
Publication number: 20140100194Abstract: 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: ApplicationFiled: December 5, 2013Publication date: April 10, 2014Applicant: Janssen Pharmaceutica, NVInventors: Raymond W Colburn, Scott L. Dax, Christopher M. Flores, Jay M. Matthews
-
Patent number: 8664204Abstract: Phosphoramidate alkylator prodrugs can be used to treat cancer when administered alone or in combination with one or more anti-neoplastic agents.Type: GrantFiled: July 12, 2013Date of Patent: March 4, 2014Assignee: Threshold Pharmaceuticals, Inc.Inventors: Mark Matteucci, Jian-Xin Duan, Hailong Jiao
-
Publication number: 20140012016Abstract: 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: ApplicationFiled: September 11, 2013Publication date: January 9, 2014Applicant: Japan Science and Technology AgencyInventors: Shu KOBAYASHI, Yasuhiro YAMASHITA, Kazutaka SEKI
-
Publication number: 20130302280Abstract: 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: ApplicationFiled: June 26, 2013Publication date: November 14, 2013Inventors: 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: 20130274484Abstract: 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: ApplicationFiled: December 24, 2010Publication date: October 17, 2013Inventors: Floryan De Campo, Tao Zhang, Changkai Zhou
-
Patent number: 8558011Abstract: 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: GrantFiled: August 31, 2010Date of Patent: October 15, 2013Assignee: Janssen Pharmaceutica, NVInventors: Raymond W Colburn, Scott L Dax, Christopher Flores, Jay M Matthews
-
Patent number: 8541397Abstract: 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: GrantFiled: February 5, 2013Date of Patent: September 24, 2013Assignee: Allergan, Inc.Inventors: Santosh C. Sinha, Smita Bhat, Evelyn Corpuz, Ken Chow, Wenkui K. Fang, Wha-Bin Im
-
Publication number: 20130217651Abstract: 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: ApplicationFiled: February 20, 2013Publication date: August 22, 2013Applicant: ALLERGAN, INC.Inventor: ALLERGAN, INC.
-
Patent number: 8507464Abstract: Phosphoramidate alkylator prodrugs can be used to treat cancer when administered alone or in combination with one or more anti-neoplastic agents.Type: GrantFiled: June 17, 2011Date of Patent: August 13, 2013Assignee: Threshold Pharmaceuticals, Inc.Inventors: Mark Matteucci, Jian-Xin Duan, Hailong Jiao, Jacob Kaizerman
-
Patent number: 8501714Abstract: 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: GrantFiled: September 7, 2010Date of Patent: August 6, 2013Assignee: 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: 20130157982Abstract: 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: ApplicationFiled: February 11, 2013Publication date: June 20, 2013Applicant: ALLERGAN, INC.Inventor: ALLERGAN, INC.
-
Publication number: 20130150331Abstract: 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: ApplicationFiled: February 5, 2013Publication date: June 13, 2013Applicant: ALLERGAN, INC.Inventor: ALLERGAN, INC.
-
Patent number: 8450501Abstract: 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: GrantFiled: November 14, 2008Date of Patent: May 28, 2013Assignee: Solvias AGInventors: Benoît Pugin, Matthias Lotz, Heidi Landert, Adrian Wyss, Raphael Aardoom, Björn Gschwend, Andreas Pfaltz, Felix Spindler
-
Publication number: 20130126792Abstract: The present invention relates to compounds of the formula (I), to the use of compounds of the formula (I) in electronic devices and electronic devices comprising one or more compounds of the formula (I). The invention furthermore relates to the preparation of the compounds of the formula (I) and to formulations comprising one or more compounds of the formula (I).Type: ApplicationFiled: July 12, 2011Publication date: May 23, 2013Applicant: Merck Patent GmbHInventors: Irina Martynova, Adam W. Franz, Christof Pflumm, Amir Hossain Parham, Arne Buesing, Rémi Manouk Anémian, Anja Gerhard
-
Patent number: 8415488Abstract: 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 radiType: GrantFiled: November 14, 2008Date of Patent: April 9, 2013Assignee: Solvias AGInventors: Benoît Pugin, Heidi Landert, Björn Gschwend, Andreas Pfaltz, Felix Spindler
-
Patent number: 8404663Abstract: 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: GrantFiled: November 28, 2011Date of Patent: March 26, 2013Assignee: Allergan, Inc.Inventors: Santosh C. Sinha, Smita S. Bhat, Evelyn G. Corpuz, Ken Chow, Wenkui K. Fang, Wha-Bin Im
-
Patent number: 8378122Abstract: The present invention is a process for the preparation of chymase modulators, useful in the treatment of inflammatory and serine protease mediated disorders.Type: GrantFiled: August 9, 2012Date of Patent: February 19, 2013Assignee: Janssen Pharmaceutica NV.Inventors: Luigi Anzalone, Penina Feibush, Ilias Konstantinos Dorziotis, Frank J. Villani
-
Publication number: 20120309986Abstract: The present invention is a process for the preparation of chymase modulators, useful in the treatment of inflammatory and serine protease mediated disorders.Type: ApplicationFiled: August 9, 2012Publication date: December 6, 2012Inventors: Luigi Anzalone, Penina Feibush, IIias Konstantinos Dorziotis, Xun Li, Frank J. Villani
-
Publication number: 20120283222Abstract: 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: ApplicationFiled: May 31, 2012Publication date: November 8, 2012Applicant: Ajinomoto Co., Inc.Inventors: Atsushi KONISHI, Munetaka Tokumasu, Tamotsu Suzuki, Takahiro Koshiba, Koji Ohsumi, Osamu Ikehara, Yuko Kodama
-
Publication number: 20120259130Abstract: The present invention is directed to an improved process for synthesizing phosphonic and phosphinic acid chymase inhibitor compounds.Type: ApplicationFiled: June 19, 2012Publication date: October 11, 2012Inventors: Luigi Anzalone, Daniel J. Pippel, Neelakandha S. Mani, Penina Feibush, IIias K. Dorziotis, Stefan Horns, Frank J. Villani, JR.
-
Publication number: 20120184510Abstract: 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: ApplicationFiled: January 14, 2011Publication date: July 19, 2012Inventors: Raymond W. Colburn, Scott L. Dax, Christopher Flores, Jay Matthews, Ning Qin, Laura Reany, Christopher Teleha, Mark A. Youngman
-
Publication number: 20120156166Abstract: 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: ApplicationFiled: September 7, 2010Publication date: June 21, 2012Applicant: 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: 8197722Abstract: 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: GrantFiled: July 30, 2001Date of Patent: June 12, 2012Assignee: The California Institute of TechnologyInventors: Seth Marder, Joseph Perry
-
Publication number: 20120142640Abstract: 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: ApplicationFiled: November 28, 2011Publication date: June 7, 2012Applicant: ALLERGAN, INC.Inventors: Santosh C. Sinha, Smita S. Bhat, Evelyn G. Corpuz, Ken Chow, Wenkui K. Fang, Wha-Bin Im
-
Publication number: 20120142805Abstract: 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: ApplicationFiled: June 29, 2010Publication date: June 7, 2012Applicant: BASF SEInventors: Hansjorg Grutzmacher, Timo Ott, Kurt Dietliker
-
Patent number: 8193372Abstract: 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: GrantFiled: March 3, 2010Date of Patent: June 5, 2012Assignee: Idenix Pharmaceuticals, Inc.Inventors: Cyril Dousson, Claire Pierra, Jean-Francois Griffon, Frederic Leroy, Jean-Laurent Paparin, David Dukhan, Dominique Surleraux
-
Publication number: 20120053347Abstract: 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: ApplicationFiled: August 31, 2010Publication date: March 1, 2012Inventors: Raymond W. Colburn, Scott L. Dax, Christopher Flores, Jay Matthews
-
Patent number: 8105504Abstract: 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: GrantFiled: August 22, 2005Date of Patent: January 31, 2012Assignee: BASF SEInventors: Michèle Gerster, Peter Nesvadba
-
Patent number: 8039496Abstract: 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: GrantFiled: January 22, 2008Date of Patent: October 18, 2011Assignee: Allergan, Inc.Inventors: David W. Old, Vinh X. Ngo
-
Publication number: 20110251159Abstract: Phosphoramidate alkylator prodrugs can be used to treat cancer when administered alone or in combination with one or more anti-neoplastic agents.Type: ApplicationFiled: June 17, 2011Publication date: October 13, 2011Applicant: Threshold Pharmaceuticals, Inc.Inventors: Mark Matteucci, Jian-Xin Duan, Hailong Jiao, Jacob Kaizerman
-
Patent number: 8030438Abstract: 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: GrantFiled: May 16, 2006Date of Patent: October 4, 2011Assignee: Nissan Chemical Industries, Ltd.Inventors: Nobuyuki Kakiuchi, Hitoshi Furusho, Naoki Otani, Tohru Minami, Tatsuo Okauchi
-
Patent number: 8003625Abstract: Phosphoramidate alkylator prodrugs can be used to treat cancer when administered alone or in combination with one or more anti-neoplastic agents.Type: GrantFiled: June 29, 2006Date of Patent: August 23, 2011Assignee: Threshold Pharmaceuticals, Inc.Inventors: Mark Matteucci, Jian-Xin Duan, Hailong Jiao, Jacob Kaizerman
-
Patent number: 7981874Abstract: 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: GrantFiled: July 16, 2007Date of Patent: July 19, 2011Assignee: 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: 20110124601Abstract: 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 substiType: ApplicationFiled: July 22, 2009Publication date: May 26, 2011Inventors: Bernard Roques, Hervé Poras, Marie-Claude Fournie-Zaluski
-
Publication number: 20110118482Abstract: 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 iType: ApplicationFiled: November 14, 2008Publication date: May 19, 2011Inventors: Benoît Pugin, Matthias Lotz, Heidi Landert, Adrian Wyss, Raphael Aardoom, Bjõrn Gschwend, Andreas Pfaltz, Felix Spindler
-
Publication number: 20110098485Abstract: 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 radiType: ApplicationFiled: November 14, 2008Publication date: April 28, 2011Inventors: Benoît Pugin, Heidi Landert, Björn Gschwend, Andreas Pfaltz, Felix Spindler
-
Publication number: 20100317625Abstract: 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: ApplicationFiled: May 21, 2007Publication date: December 16, 2010Inventors: 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: 20100279983Abstract: 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: ApplicationFiled: May 21, 2007Publication date: November 4, 2010Inventors: 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: 20100233123Abstract: 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: ApplicationFiled: March 3, 2010Publication date: September 16, 2010Applicant: Idenix Pharmaceuticals, Inc.Inventors: Cyril Dousson, Claire Pierra, Jean-Francois Griffon, Frederic Leroy, Jean-Laurent Paparin, David Dukhan, Dominique Surleraux
-
Patent number: 7763739Abstract: 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: GrantFiled: April 14, 2005Date of Patent: July 27, 2010Assignee: Evonik Degussa, GmbHInventors: Renat Kadyrov, Juan José Almena Perea, Axel Monsees, Thomas Riermeier, Ilias Ilaldinov
-
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