The Phosphorus Is Part Of A Substituent Which Is Attached Directly To Ring Carbon Of The Five-membered Hetero Ring Patents (Class 548/119)
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Publication number: 20110118472Abstract: The present invention belongs to a spiro phosphine-oxazoline and preparation method and application thereof, particularly, publishes a novel spiro phosphine-oxazoline and the preparation method of its iridium complex. The substituted 7-diaryl phosphino-7?-carboxy-1,1?-Lo-dihydro-indene is used as the starting raw material to synthesize the novel spiro phosphine-oxazoline of the present invention through a two-step reaction. The novel spiro phosphine-oxazoline and the iridium precursor are complexed to become a complex, and then through ion exchange, an iridium/phosphine spiro-oxazoline complex with different anions can be obtained. The present invention overcomes the shortcomings of the existing technology. The cheap readily available amino alcohol is used as the raw material to synthesize the novel spiro phosphine-oxazoline, on the fourth position of the oxazoline ring of which there is no substitutent.Type: ApplicationFiled: January 20, 2009Publication date: May 19, 2011Applicant: Zheijiang Jiuzhou Pharmaceutical Co., Ltd.Inventors: Qilin Zhou, Shoufej Zhu, Shen Li, Lixin Wang, Song Song
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Publication number: 20110105749Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.Type: ApplicationFiled: June 14, 2010Publication date: May 5, 2011Inventors: Weiwen YING, David James, Shijie Zhang, Teresa Przewloka, Junghyun Chae, Dinesh U. Chimmanamada, Chi-Wan Lee, Elena Kostik, Howard P. Ng, Kevin Foley, Zhenjian Du, James Barsoum
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Publication number: 20110064698Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention relates to novel antiviral compounds represented herein above, pharmaceutical compositions comprising such compounds, and methods for the treatment or prophylaxis of viral (particularly HCV) infection in a subject in need of such therapy with said compounds.Type: ApplicationFiled: September 10, 2010Publication date: March 17, 2011Inventors: Yat Sun Or, Xiaowen Peng, Ce Wang, Lu Ying, Yao-Ling Qiu
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Publication number: 20110059964Abstract: The present invention relates to the orexin receptor antagonists compounds of the general formula (I) as well as to their isomers, salts and solvates, to the pharmaceutical compositions containing them and to the therapeutic application thereof.Type: ApplicationFiled: February 3, 2010Publication date: March 10, 2011Applicant: sanofi-aventisInventors: Michel Aletru, Peter Aranyi, Maria Balogh, Sandor Batori, Judit Bence, Philippe Bovy, Zoltan Kapui, Endre Mikus, Claudie Namane, Christophe Philippo, Tibor Szabo, Zsuzsanna Tomoskozi, Katalin Urban-Szabo
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Publication number: 20110059893Abstract: The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, and prodrug thereof, wherein Ra, Rb, and R2 are defined herein. These compounds inhibit tubulin polymerization and/or target vasculature and are useful for treating proliferative disorders, such as cancer.Type: ApplicationFiled: September 16, 2010Publication date: March 10, 2011Inventors: Lijun Sun, Christopher Borella, Hao Li, Jun Jiang, Shoujun Chen, Keizo Koya, Takayo Inoue, Zhenjian Du, Kevin Foley, Yaming Wu, Mei Zhang, Weiwen Ying
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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
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Publication number: 20100292084Abstract: A novel process of preparing tridentate ligands containing one or more of a diarylphosphine and/or dialkylphosphine electron donating groups are disclosed. Use of this process for preparing a combinatorial library of such tridentate ligands and of organometallic complexes containing same is also disclosed. Further disclosed are novel diarylphosphine-containing and dialkylphosphine-containing compounds that can serve as tridentate ligands (e.g., pincer ligands), combinatorial libraries of such tridentate ligands, organometallic complexes containing these ligands (e.g., pincer complexes), and combinatorial libraries of such complexes. Methods utilizing these libraries for screening for candidate organometallic catalysts are also disclosed. Novel precursor molecules useful for preparing the tridentate ligands and processes of preparing same are also disclosed.Type: ApplicationFiled: May 13, 2010Publication date: November 18, 2010Applicant: Technion Research & Development Foundation Ltd.Inventors: Mark GANDELMAN, Elaine Melissa Schuster, Gennady Nisnevich
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Publication number: 20100292190Abstract: The present invention relates to compounds of general formula (I) as tublin polymerisation inhibitors and methods for preparing such compounds.Type: ApplicationFiled: February 14, 2006Publication date: November 18, 2010Applicant: Bionomics LimitedInventors: Jason Hugh Chaplin, Gurmit Singh Gill, Damian Wojciech Grobelny, Bernard Luke Flynn
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Publication number: 20100292100Abstract: A novel process of preparing tridentate ligands containing a diarylphosphine electron donating group are disclosed. Use of this process for preparing a combinatorial library of such tridentate ligands and of organometallic complexes containing same is also disclosed. Further disclosed are novel diarylphosphine-containing compounds that can serve as tridentate ligands (e.g., pincer ligands), combinatorial libraries of such tridentate ligands, organometallic complexes containing these ligands (e.g., pincer complexes), and combinatorial libraries of such complexes. Methods utilizing these libraries for screening for candidate organometallic catalysts are also disclosed.Type: ApplicationFiled: May 14, 2009Publication date: November 18, 2010Applicant: Technion Research & Development Foundation Ltd.Inventors: Mark GANDELMAN, Elaine Melissa SCHUSTER
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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
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Publication number: 20100273744Abstract: The present invention relates to amide compounds, processes for their preparation, pharmaceutical compositions containing these compounds and to their use in the treatment of disorders, conditions or disorders such as allergic disorders, inflammatory disorders and disorders of the immune system.Type: ApplicationFiled: April 22, 2010Publication date: October 28, 2010Inventors: Paul Martin Gore, Steven Leslie Sollis
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Publication number: 20100261677Abstract: The invention relates to substituted arylsulphonylaminomethylphosphonic acid derivatives of general formula (I) wherein the groups Ra to Rf, A and Z are defined as mentioned in the specification and claims, which are suitable for preparing a medicament for the treatment of metabolic disorders, particularly type 1 or type 2 diabetes mellitus.Type: ApplicationFiled: September 4, 2008Publication date: October 14, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Elke Langkopf, Alexander Pautsch, Corinna Schoelch, Annette Schuler-Metz, Ruediger Streicher, Holger Wagner
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Publication number: 20100261673Abstract: Embodiments of the present invention provide novel antibacterials that target penicillin-binding proteins or other important cellular targets. Methods for inhibiting growth (reproduction, etc.) of bacteria using compounds described herein are also provided. Various embodiments exhibit activity against gram positive bacteria, such as certain strains of Entercoccus and Staphylococcus aureus.Type: ApplicationFiled: December 21, 2007Publication date: October 14, 2010Applicant: UNIVERSITY OF NOTRE DAME DU LACInventors: Shahriar Mobashery, Peter I. O'Daniel, Mayland Chang
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Publication number: 20100249426Abstract: It is an object of the present invention to provide a pharmaceutical composition containing a stable azole-based compound, which is useful as an antifungal agent. According to the present invention, the above-mentioned object can be achieved by adding magnesium hydroxide carbonate, triethylamine, arginine, or another such basic substance to an azole-based compound that is unstable in acids. The above-mentioned pharmaceutical composition is stable enough that the compound will not degrade if the temperature, humidity, or other such conditions should change during production or storage. Also, this composition is useful as a therapeutic agent for deep mycoses because systemic administration is possible by applying it to an oral agent or an injection.Type: ApplicationFiled: February 22, 2007Publication date: September 30, 2010Inventors: Hayato Ishimoto, Tsutomu Harada, Hiroshi Omae
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Publication number: 20100249071Abstract: The invention is directed to Compounds of Formula I: as well as methods of making and using the compounds.Type: ApplicationFiled: March 25, 2010Publication date: September 30, 2010Applicant: Exelixis, Inc.Inventors: Lynne Canne Bannen, Diva Sze-Ming Chan, Morrison B. Mac, Stephanie Ng, John M. Nuss, Yong Wang, Wei Xu
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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
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Publication number: 20100186961Abstract: Novel aminoacid alkylphosphonic acid compounds are disclosed. These compounds can be used in multiple applications, in particular in a scale inhibitor functionality in aqueous systems, including in marine oil recovery.Type: ApplicationFiled: May 25, 2007Publication date: July 29, 2010Inventors: Patrick Notte, Albert Devaux
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Publication number: 20100137254Abstract: Phosphoramidate alkylator prodrugs can be used to treat cancer when administered along or in combination with one or more anti-neoplastic agents.Type: ApplicationFiled: June 29, 2006Publication date: June 3, 2010Inventors: Mark Matteucci, Jian-Xin Duan, Hailong Jiao
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Publication number: 20100137243Abstract: Compounds of Formula (I), or a pharmaceutically-acceptable salt, or an in-vivo-hydrolysable ester thereof, and compounds as shown in Formula (I) wherein C is for example (D), (E), (F); wherein A and B are independently selected from (i) and (ii); R2a to R3b are independently selected from hydrogen and fluorine; R1a and R1b are independently selected from, for example, hydroxy, —NHC(?W)R4, (a) and (b); wherein W is O or S; R4 is, for example, hydrogen, amino, (1-4C)alkyl; HET-1 is, for example, a C-linked 5-membered heteroaryl ring; HET-2 is, for example, an N-linked 5-membered, fully or partially unsaturated heterocyclic ring; are useful as antibacterial agents; and processes for their manufacture and pharmaceutical compositions containing them are described.Type: ApplicationFiled: May 28, 2008Publication date: June 3, 2010Applicant: AstraZeneca ABInventors: Michael Barry Gravestock, Neil James Hales, Michael Lingrad Swaim, Sheila Irene Hauck, Stuart Dennett Mills
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Patent number: 7723542Abstract: The invention relates to a process for the preparation of diphosphonic acids by reaction of a carboxylic acid with a mixture of phosphorous acid and phosphorus oxychloride in defined molar ratios and in the absence of solvents. The invention further relates to ibandronic acid monosodium salt in the amorphous form.Type: GrantFiled: December 22, 2004Date of Patent: May 25, 2010Assignee: Trifarma S.p.A.Inventors: Simona Grassi, Anna Volante
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Patent number: 7718633Abstract: A compound of the formula is disclosed as a prodrug of an HIV protease inhibitor. Methods and compositions for inhibiting HIV protease activity and treating HIV infection are also disclosed.Type: GrantFiled: June 29, 2005Date of Patent: May 18, 2010Assignee: Abbott LaboratoriesInventors: David A. DeGoey, William J. Flosi, David J. Grampovnik, Larry L. Klein, Dale J. Kempf, Xiu C. Wang
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Publication number: 20100113542Abstract: 5-[4-(2-Methylphenyl)-3-hydroxy-4H-1,2,4-triazol-5-yl]-2,4-dihydroxy-N-methyl-N-butylbenzamide is an HSP90 inhibitor and can be used for the preparation of a medicament for the treatment of diseases in which the inhibition, regulation and/or modulation of HSP90 plays a role.Type: ApplicationFiled: December 11, 2007Publication date: May 6, 2010Applicant: Merck Patent GesellschaftInventors: Hans-Michael Eggenweiler, Michael Wolf, Hans Peter Buchstaller, Christian Sirrenberg
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Publication number: 20100009936Abstract: The invention provides compounds formula I, their preparation, and their use as pharmaceutically active immuno-suppressive agents for the treatment of autoimmune disorders, organ transplant rejection, disorders associated with an activated immune system, as well as other disorders modulated by lymphopenia or SIP receptors.Type: ApplicationFiled: August 1, 2007Publication date: January 14, 2010Applicant: PRAECIS PHARMACEUTICALS INCORPORATEDInventors: Ghotas Evindar, Hongfeng Deng, Sylvie Bernier, Gang Yao, Aaron Coffin, Hongfang Yang
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Publication number: 20090326227Abstract: A process for the preparation of biphosphonic acids and pharmaceutical acceptable salts thereof, comprises reacting a carboxylic acid with phosphorous trichloride and phosphorous acid in the presence of an aprotic polar solvent.Type: ApplicationFiled: November 6, 2007Publication date: December 31, 2009Applicant: HOVIONE INTER LIMITEDInventors: Joana Baptista, Zita Mendes
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Publication number: 20090318389Abstract: The invention provides compounds formulae I-III, their preparation, and their use as pharmaceutically active immunosuppressive agents for the treatment of autoimmune disorders, organ transplant rejection, disorders associated with an activated immune system, as well as other disorders modulated by lymphopenia or SIP receptors.Type: ApplicationFiled: August 2, 2007Publication date: December 24, 2009Applicant: PRAECIS PHARMACEUTICALS INCORPORATEDInventors: Ghotas Evindar, Hongfeng Deng
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Publication number: 20090304605Abstract: The invention provides amino-substituted aminothiazole compounds of Formula I and Formula II where A is a group of the formula: and the variables X, Y, R, and R1 to R7 are described herein. These compounds are prodrugs of compounds useful as inhibitors of viral replication. Compositions containing such compounds, and methods of treating viral infections with these compounds, as well as to processes and intermediates useful for preparing such compounds are also provided by the invention.Type: ApplicationFiled: June 5, 2009Publication date: December 10, 2009Applicant: ACHILLION PHARMACEUTICALS, INC.Inventors: Cuixan Liu, Avinash Phadke, Xiangzhu Wang, Suoming Zhang
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Publication number: 20090274972Abstract: An electrostatic-image-developing toner includes a phosphonic acid based sequestering agent.Type: ApplicationFiled: December 15, 2008Publication date: November 5, 2009Applicant: FUJI XEROX CO., LTD.Inventors: Shuji SATO, Eisuke IWAZAKI, Atsushi SUGAWARA, Masanobu NINOMIYA, Hiroshi NAKAZAWA
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Publication number: 20090208499Abstract: The present invention relates to an N-(phosphonoalkyl)-amino acid, a related compound or a derivative thereof, the N-(phosphonoalkyl)-amino acid, related compound or derivative thereof being in a form as a free acid, salt, partial salt, lactone, amide or ester, or in stereoisomeric or non-stereoisomeric form, other than N-(phosphonomethyl)-glycine or N,N-bis(phosphonomethyl)-glycine. Also included is a composition including an N-(phosphonoalkyl)-amino acid, a related compound or a derivative thereof in a form as a free acid, salt, partial salt, lactone, amide or ester, or in stereoisomeric or non-stereoisomeric form, and a cosmetically or pharmaceutically acceptable vehicle for topical or systemic administration to a mammalian subject, as well as a method of administering an effective amount of such a composition for alleviating or improving a condition, disorder, symptom or syndrome associated with at least one of a nervous, vascular, musculoskeletal or cutaneous system.Type: ApplicationFiled: April 23, 2009Publication date: August 20, 2009Inventors: Ruey J. Yu, Eugene J. Van Scott
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Patent number: 7576198Abstract: A compound of the formula (I): wherein X is hydroxy or the like; Y is —C(?R2)—R3—R4 wherein R2 and R3 is oxygen atom or the like, R4 is hydrogen, optionally substituted alkyl, optionally substituted heteroaryl or the like; Z is hydrogen or the like; Z1 and Z3 each is independently a bond, alkylene or the like; Z2 is a bond, alkylene, —O— or the like; R1 is optionally substituted aryl, optionally substituted heteroaryl or the like; p is 0 to 2 and ring (A) is optionally substituted aromatic heterocycle, a tautomer of itself, a prodrug thereof, a pharmaceutically acceptable salt thereof or a solvate thereof has an integrase-inhibiting activity.Type: GrantFiled: August 25, 2000Date of Patent: August 18, 2009Assignee: Shionogi & Co., Ltd.Inventors: Takashi Kawasuji, Tomokazu Yoshinaga
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Publication number: 20090192316Abstract: An object of the present invention is to provide a process, or the like, suitable for the industrialization of effective deprotection reaction without using a toxic solvent as well as to provide a process, or the like, for preparing a water-soluble azole prodrug effectively. The present invention provides a process for preparing a salt represented by Formula (I); (wherein X represents a fluorine atom bonded at position 4 or position 5 of a phenyl group) comprising the steps of: (a) carrying out a deprotection reaction of a compound represented by Formula (II); (wherein X represents a fluorine atom bonded at position 4 or position 5 of a phenyl group) in the presence of a carbocation scavenger.Type: ApplicationFiled: December 20, 2006Publication date: July 30, 2009Inventors: Manabu Sasho, Keizo Sato, Jun Niijima, Mamoru Miyazawa, Shigeto Negi, Atsushi Kamada
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Publication number: 20090186834Abstract: Various azetidinone, pyrrolidine, imidazolidine, and oxazolidine derivatives are described, as are pharmaceutical compositions containing these compounds and methods of treatment of diseases using these compounds. Other embodiments are also described.Type: ApplicationFiled: March 24, 2006Publication date: July 23, 2009Applicant: MICROBIA, INC.Inventors: John Talley, Eduardo Martinez, Daniel Zimmer, Regina Lundrigan
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Publication number: 20090186891Abstract: The present invention provides compounds of the following structure; A-Q-B—C-D that are useful for treating conditions or disorders associated with DGAT1 activity in animals, particularly humans.Type: ApplicationFiled: September 26, 2008Publication date: July 23, 2009Inventors: Young-Shin Kwak, Gary Mark Coppola
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Patent number: 7557095Abstract: Disclosed herein is a compound having a structure or a pharmaceutically acceptable salt thereof, or a prodrug thereof. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.Type: GrantFiled: May 7, 2007Date of Patent: July 7, 2009Assignee: Allergan, Inc.Inventors: Robert M. Burk, David W. Old, Todd Gac
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Patent number: 7550448Abstract: Disclosed herein is a compound having a structure or a pharmaceutically acceptable salt, or a prodrug thereof. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.Type: GrantFiled: May 11, 2007Date of Patent: June 23, 2009Assignee: Allergan, Inc.Inventors: David W. Old, Danny T. Dinh
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Patent number: 7538228Abstract: A chiral ligand represented by the formula and its enantiomer: wherein A, X, Y and Z are as defined in the specification is provided. Also provided is a process of making the chiral ligands and catalysts prepared from these ligands and a transition metal, a salt thereof or a complex thereof. In addition, a method of preparing an asymmetric compound by a transition metal catalyzed asymmetric reaction, such as, hydrogenation, hydride transfer reaction, hydrosilylation, hydroboration, hydrovinylation, hydroformylation, hydrocarboxylation, allylic alkylation, epoxidation, cyclopropanation, Diels-Alder reaction, Aldol reaction, ene reaction, Heck reaction and Michael addition is provided.Type: GrantFiled: December 17, 2004Date of Patent: May 26, 2009Assignee: The Penn State Research FoundationInventors: Xumu Zhang, Duan Liu
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Publication number: 20090105481Abstract: Process for stereoselective hydrogenation by reacting racemic aldehydes or ketones having a stereogenic carbon atom in the position relative to the C(O) group and containing the structural element —(O)C—C—CH— by means of hydrogen in the presence of a base and a ruthenium complex containing a bidentate ligand having coordinating P and N atoms, a monophosphine ligand and anionic and/or uncharged ligands as homogeneous catalyst, with the charge being balanced by one or two monovalent acid anions or a divalent acid anion when uncharged ligands are present.Type: ApplicationFiled: March 8, 2007Publication date: April 23, 2009Inventors: Felix Spindler, Ulrike Nettekoven, Mauro Perseghini
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Patent number: 7514556Abstract: The intention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel ?-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic ?-lactamase inhibitors presently available, and which do not require a ?-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.Type: GrantFiled: July 30, 2007Date of Patent: April 7, 2009Assignee: Methylgene Inc.Inventors: Jeffrey M. Besterman, Jubrail Rahil, Arkadii Vaisburg
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Publication number: 20090060872Abstract: Provided herein are phosphadiazine polymerase inhibitor, for example, of any of Formulas V, V?, I?, II?, or Va, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.Type: ApplicationFiled: August 27, 2008Publication date: March 5, 2009Applicant: Idenix Pharmaceuticals, Inc.Inventors: Cyril Dousson, Dominique Surleraux, Jean-Laurent Paparin
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Publication number: 20090011975Abstract: The invention provides a method of inhibiting cell death in a mammal. The method comprises administering to a mammal an effective amount of a composition comprising a cell protection factor covalently linked to a bone targeting agent via a linkage that is cleaved under physiological conditions, whereby the cell protection factor is released from the bone targeting agent in vivo to inhibit cell death. The invention further provides a compound comprising a cell protection factor covalently attached to a bone targeting agent via a linker that is cleaved under physiological conditions.Type: ApplicationFiled: July 31, 2008Publication date: January 8, 2009Applicant: Semafore Pharmaceuticals Inc.Inventors: Joseph R. Garlich, Donald L. Durden, Tim C. Smith
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Patent number: 7439385Abstract: The present invention provides a novel process for preparation of bisphosphonic acid derivatives or pharmaceutical acceptable salt thereof, by reacting carboxylic acid having structural formula (II) with phosphorous acid and a halophosphorous compound, wherein halophosphorous compound is selected from the group comprising of PCl3, PCl5, POCl3, PBr3, POBr3, and PBr5 in presence of diphenyl ether.Type: GrantFiled: July 24, 2006Date of Patent: October 21, 2008Assignee: Alembic LimitedInventors: Pandurang Balwant Deshpande, Parven Kumar Luthra
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Publication number: 20080221335Abstract: The invention relates to a method for the manufacture of substituted phosphanes and substituted phosphanes manufactured according to the method. Phosphanes, phosphane oxides, sulfides or selenides are used as ligands in coordination compounds. They play a central role in controlling the activity and selectivity of catalysts. The object is achieved by the invention by synthesizing heterocyclic substituents on aromatic groups by introducing acetyl groups. In this manner, previously unknown representatives of the families of phosphanes, phosphane oxides, sulfides and selenides are made accessible.Type: ApplicationFiled: October 17, 2005Publication date: September 11, 2008Inventors: Werner Thiel, Yu Sun, Antje Hienzsch
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Patent number: 7411087Abstract: The present invention provides a novel process for preparation of bisphosphonic acids or salts thereof, e.g. alendronic acid, by reacting a carboxylic acid, phosphorous acid and a halophosphorous compound in a water miscible neutral solvent.Type: GrantFiled: August 10, 2004Date of Patent: August 12, 2008Assignee: Sun Pharmaceutical Industries LimitedInventors: Vijaykumar Muljibhai Patel, Trinadha Rao Chitturi, Rajamannar Thennati
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Publication number: 20080009465Abstract: Compounds are provided which are phosphonate and phosphinate activators and thus are useful in treating diabetes and related diseases and have the structure wherein is a heteroaryl ring; R4 is —(CH2)n-Z-(CH2)m—PO(OR7)(OR8), —(CH2)nZ-(CH2)m—PO(OR7)Rg, —(CH2)n-Z-(CH2)m—OPO(OR7)Rg, —(CH2)nZ—(CH2)m—OPO(R9)(R10), or —(CH2)nZ—(CH2)m—PO(R9)(R10); R5 and R6 are independently selected from H, alkyl and halogen; Y is R7(CH2)s or is absent; and X, n, Z, m, R4, R5, R6, R7, and s are as defined herein; or a pharmaceutically acceptable salt thereof. A method for treating diabetes and related diseases employing the above compounds is also provided.Type: ApplicationFiled: June 28, 2007Publication date: January 10, 2008Inventors: Denis E. Ryono, Peter T.W. Cheng, Scott A. Bolton, Sean Chen, Yan Shi, Wei Meng, Joseph A. Tino, Hao Zhang, Richard B. Sulsky
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Patent number: 7312219Abstract: Novel FBPase inhibitors of the formula I and X are useful in the treatment of diabetes and other conditions associated with elevated blood glucose.Type: GrantFiled: August 6, 2003Date of Patent: December 25, 2007Assignee: Metabasis Therapeutics, Inc.Inventors: Qun Dang, Srinivas Rao Kasibhatla, K. Raja Reddy, Mark D. Erion, M. Rami Reddy, Atul Agurwal
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Patent number: 7129350Abstract: A process for the preparation of 3-cyclic-ether-substituted cephalosporins of formula I wherein the group CO2R1 is a carboxylic acid or a carboxylate salt and R2 has the formula: wherein A1 and A2 have the meanings given in the specification by reacting compound of formula II: wherein R2 is as defined above and R3 is para-nitrobenzyl or allyl with a compound R2 L wherein R2 is as defined above; and L is di-(C1-6 alkyl)phosphorothioate in the presence of a solvent and a base.Type: GrantFiled: February 11, 2004Date of Patent: October 31, 2006Assignee: Pfizer, Inc.Inventors: Juan C. Colberg, Maurizio Zenoni, Giovanni Fogliato, Alessandro Donadelli
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Patent number: 7105556Abstract: Compounds are provided which have the structure wherein Q is C or N, X1 is C or N, and R1, R2, R2a, R2b, R2c, R3, Y, A, m, n, X2, X3 and X4 are as defined herein, which compounds are useful as antidiabetic, hypolipidemic, and antiobesity agents.Type: GrantFiled: May 22, 2002Date of Patent: September 12, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Peter T. Cheng, Yoon Jeon, Wei Wang
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Patent number: 7060290Abstract: Disclosed are compounds of general formula (I) that function as prodrugs, thereby increasing bioavailabilities of the linked therapeutic agents, wherein the LINKER is (i) substituted or unsubstituted alkyl, (ii) substituted or unsubstituted alkenyl, (iii) substituted or unsubstituted alkanoyl, (iv) substituted or unsubstituted alkenoyl wherein the double bond is cis, and (v) (ortho or para) carbonyl-substituted aryl; and wherein the subtituent is each an independent group or linked together thereby forming a ring; and wherein X is one or more substituted or unsubstituted group containing one or more O, N, or S atom and wherein the substituent is each an independent group or linked together thereby forming a ring; and wherein the therapeutic agent is an alcohol-containing water-insoluble steroids or another alcohol containing compounds and methods to prepare such compounds.Type: GrantFiled: February 16, 2000Date of Patent: June 13, 2006Assignee: Supergen, Inc.Inventors: Bruce H. Morimoto, Peter L. Barker
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Patent number: 6982336Abstract: A 1,2-dioxetane derivative of the formula (I): wherein R1–R3 and Ar are defined in the claims is provided.Type: GrantFiled: March 7, 2002Date of Patent: January 3, 2006Assignee: Tosoh CorporationInventors: Masakatsu Matsumoto, Nobuko Watanabe, Masashi Yamada
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Patent number: 6965033Abstract: Novel bisamidate phosphonate prodrugs of FBPase inhibitors of the Formula IA: and their use in the treatment of diabetes and other conditions associated with elevated blood glucose.Type: GrantFiled: December 22, 2000Date of Patent: November 15, 2005Assignee: Metabasis Therapeutics, Inc.Inventors: Tao Jiang, Srinivas Rao Kasibhatla, K. Raja Reddy
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Patent number: 6838474Abstract: The present invention relates to prodrugs of a class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of prodrugs of HIV aspartyl protease inhibitors characterized by favorable aqueous solubility, high oral bioavailability and facile in vivo generation of the active ingredient. This invention also relates to pharmaceutical compositions comprising these prodrugs. The prodrugs and pharmaceutical compositions of this invention are particularly well suited for decreasing the pill burden and increasing patient compliance. This invention also relates to methods of treating mammals with these prodrugs and pharmaceutical compositions.Type: GrantFiled: February 19, 2003Date of Patent: January 4, 2005Assignee: Vertex Pharmaceuticals, IncorporatedInventors: Roger Dennis Tung, Michael Robin Hale, Christopher Todd Baker, Eric Steven Furfine, Istvan Kaldor, Wieslaw Mieczylaw Kazmierski, Andrew Spaltenstein