Chalcogen Bonded Directly To The Oxazine Ring Patents (Class 544/97)
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Publication number: 20100240622Abstract: The invention provides compositions and kits comprising at least one nitric oxide enhancing prostaglandin compound or a pharmaceutically acceptable salt thereof, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating ophthalmic disorders; (b) treating cerebrovascular disorders; (c) treating cardiovascular disorders; (d) treating benign prostatic hyperplasia (BPH); (e) treating peptic ulcers; (e) treating sexual dysfunctions and (f) inducing abortions. The nitric oxide enhancing prostaglandin compounds comprise at least one heterocyclic nitric oxide donor group and/or at least one nitroxide group.Type: ApplicationFiled: March 19, 2007Publication date: September 23, 2010Applicant: NITROMED, INC.Inventor: David S. Garvey
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Patent number: 7795251Abstract: The present invention relates 3,4-dihydro-benzo[e][1,3]oxazin-2-ones which are substituted at the nitrogen atom by unsubstituted or substituted (C1-8)alkyl, (C3-8)cycloalkyl, (C3-8)cycloalkyl(C1-4)alkyl, (C6-18)aryl or (C6-18)aryl(C1-4)alkyl and their use as pharmaceuticals.Type: GrantFiled: April 13, 2006Date of Patent: September 14, 2010Assignee: Novartis AGInventors: Andreas Billich, Hubert Gstach, Philipp Lehr
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Publication number: 20100197675Abstract: This invention relates to novel compounds of the Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11 ?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of Cortisol in a cell or the inhibition of the conversion of cortisone to Cortisol in a cell.Type: ApplicationFiled: February 26, 2008Publication date: August 5, 2010Inventors: David A. Claremon, Gerard McGeehan, Suresh B. Singh, Colin M. Tice, Yuanjie Ye, Wei Zhao
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Patent number: 7767811Abstract: One aspect of the present invention relates to a method for the kinetic resolution of racemic and diastereomeric mixtures of chiral compounds. The critical elements of the method are: a non-racemic chiral tertiary-amine-containing catalyst; a racemic or diastereomeric mixture of a chiral substrate, e.g., a cyclic carbonate or cyclic carbamate; and a nucleophile, e.g., an alcohol, amine or thiol. A preferred embodiment of the present invention relates to a method for achieving the kinetic resolution of racemic and diastereomeric mixtures of derivatives of ?- and ?-amino, hydroxy, and thio carboxylic acids. In certain embodiments, the methods of the present invention achieve dynamic kinetic resolution of a racemic or diastereomeric mixture of a substrate, i.e.Type: GrantFiled: June 5, 2006Date of Patent: August 3, 2010Assignee: Brandeis UniversityInventors: Li Deng, Jianfeng Hang, Liang Tang
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Publication number: 20100173889Abstract: Substituted pyrimidine and triazine compounds corresponding to formula I wherein R1, R2, R3, R4a, R4b, R5a, R5b, R7, R8, R9a, R9b, R10, R11, A, a, b, s, t, V, W1, W2 and W3 have defined meanings, pharmaceutical compositions comprising such compounds, a process for preparing such compounds, and the use of such compounds and compositions to treat or inhibit pain and/or other disorders or disease states.Type: ApplicationFiled: October 23, 2009Publication date: July 8, 2010Applicant: GRUENENTHAL GmbHInventors: Stefan Schunk, Melanie Reich, Kamila Hennig, Michael Engels, Tieno Germann, Ruth Jostock, Sabine Hees
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Publication number: 20100035865Abstract: The invention is directed to a class of compounds, including the pharmaceutically acceptable salts of the compounds, having the structure of formula (I), as defined in the specification. The invention is also directed to compositions containing the compounds of formula (I).Type: ApplicationFiled: March 26, 2008Publication date: February 11, 2010Inventors: Kimberly Gail Estep, Anton F.J. Fliri, Christopher J. O'Donnell
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Patent number: 7659300Abstract: The present invention is directed to compounds of Formula I: I (where A1, A2, B, J, K, m, n, R4, R5a, R5b and R5c are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.Type: GrantFiled: September 6, 2005Date of Patent: February 9, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Ian M. Bell, Craig A. Stump
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Publication number: 20100016164Abstract: A haloalkylsulfonanilide derivative represented by general formula (I) or a salt thereof wherein R1 represents a halo(C1-C8)alkyl group, R2, R3, R4, R5, R6, R7, R8, R9 and R10 represent hydrogen atoms, etc., n represents 1 or 2, A represents an oxygen atom, W represents an oxygen atom, X represents a halogen atom and m represents an integer of 0 to 4, are compounds useful as herbicides having both of remarkable herbicidal effect and characteristics such as excellent crop-weed selectivity.Type: ApplicationFiled: November 16, 2007Publication date: January 21, 2010Inventors: Tomokazu Hino, Yasuko Yamada, Toshihiko Shigenari, Koki Mametsuka
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Publication number: 20090270395Abstract: This invention relates to potent selective agonists of the EP4 subtype of prostaglandin E2 receptors, their use or a formulation thereof in the treatment of glaucoma and other conditions, which are related to elevated intraocular pressure in the eye of a patient. This invention further relates to the use of the compounds of this invention for mediating the bone modeling and remodeling processes of the osteoblasts and osteoclasts. The compounds of the present invention are the compounds of Formula (I).Type: ApplicationFiled: July 28, 2006Publication date: October 29, 2009Inventors: John Colucci, Yongxin Han, Julie A. Farand
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Patent number: 7598241Abstract: Novel compounds of the formula (I) in which R1, D, X, W, Y and T have the meaning indicated in Patent Claim (1), e.g. (II), are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic diseases and for the treatment of tumors.Type: GrantFiled: January 8, 2004Date of Patent: October 6, 2009Assignee: Merck Patent GmbHInventors: Dieter Dorsch, Bertram Cezanne, Werner Mederski, Christos Tsaklakidis, Johannes Gleitz, Christoph van Amsterdam
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Publication number: 20090187017Abstract: The present invention relates to a process for the organo-catalysed kinetic racemate resolution of compounds of the general formula (II). It is thus possible through the action of catalytic amounts of enantiomerically enriched compounds of the general formula (Ia) or (Ib) to obtain on the one hand enantiomerically enriched optionally N-acylated ?-amino acid esters and on the other hand enantiomerically enriched 4,5-dihydrooxazin-6-ones (oxazinones). The corresponding enantiomerically enriched ?-amino acids can be formed from both easily separable classes of compounds by simple hydrolysis.Type: ApplicationFiled: July 25, 2006Publication date: July 23, 2009Applicant: Evonik Degussa GmbHInventors: Albrecht Berkessel, Felix Cleemann, Santanu Mukherjee
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Publication number: 20090069309Abstract: Compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof is disclosed herein. A, X, J, E, and Z are as described herein. These compounds are useful for treating diseases.Type: ApplicationFiled: August 14, 2008Publication date: March 12, 2009Applicant: ALLERGAN, INC.Inventors: David W. Old, Danny T. Dinh
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Publication number: 20090048240Abstract: This invention provides compositions which are 1,3-oxazinan-2-one compounds of formulae (I) and (II), and oxazolidinone compounds of formula (III): wherein R is a hydrocarbyl group, a heterocyclic group, a hydrocarbyl group having at least one substituent, or a heterocyclic group having at least one hydrocarbyl substituent, wherein the substituent on the hydrocarbyl group or heterocyclic group is selected from the group consisting of a heterocyclic group, an azo group, a cyano group, a nitro group, a fluoro group, a chloro group, a bromo group, an alkoxy group having up to 15 carbon atoms, and a hydrocarbyl group having up to 15 carbon atoms; and R? and R? are each independently hydrogen, an alkyl group, an aryl group, a methylaryl group, a carbonyl group, a hydrocarbylamido group, a sulfonyl group, a sulfonamoyl group, a heterocyclic group, a heterocyclic group having at least one substituent, or an aryl group or methylaryl group having at least one substituent, where the substituent on the heterocyclic grouType: ApplicationFiled: February 9, 2007Publication date: February 19, 2009Applicant: University of New Orleans Research & Technology FoundationInventor: Guijun Wang
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Publication number: 20090018054Abstract: Compounds of Formula (I), including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In the compounds of Formula (I), A1 is a cyclic group, and B is a cyclic group which is attached to the heterocyclic ring directly or through a methylene group.Type: ApplicationFiled: December 29, 2006Publication date: January 15, 2009Inventors: Amjad Ali, Peter J. Sinclair, Gayle E. Taylor
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Patent number: 7427614Abstract: Compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof is disclosed herein. A, X, J, E, and Z are as described herein. These compounds are useful for treating diseases.Type: GrantFiled: June 2, 2005Date of Patent: September 23, 2008Assignee: Allergan, Inc.Inventors: David W. Old, Danny T. Dinh
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Patent number: 7399760Abstract: Pyrimidinedione derivatives of the general formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them are useful for the treatment of inflammation and immunological diseases.Type: GrantFiled: May 1, 2006Date of Patent: July 15, 2008Assignee: Bexel Pharmaceuticals Inc.Inventors: Shiv Kumar Agarwal, Ravikumar Tadiparthi, Pawan Aggarwal, Savithiri Shivakumar
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Patent number: 7279582Abstract: A compound of the formula: is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.Type: GrantFiled: October 25, 2002Date of Patent: October 9, 2007Assignee: Abbott LaboratoriesInventors: Eric J. Stoner, Arthur J. Cooper, Lawrence Kolaczkowski, Ketan M. Patel, Hing Leung Sham, Daniel W. Norbeck, Xiaoqi Chen, David A. Betebenner, Thomas R. Herrin, Gondi N. Kumar, Stephen L. Condon, Daniel A. Dickman, Patricia A. Oliver, Jien-Heh J. Tien
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Patent number: 7094778Abstract: This invention relates to compounds which are generally muscarinic M2/M3 receptor antagonists and which are represented by Formula I: wherein X, Y, and Z are O, S or NR5, and the other substituents are as defined in the specification; and prodrugs, individual isomers, racemic or non-racemic mixtures of isomers, and pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds and methods for their use as therapeutic agents.Type: GrantFiled: October 14, 2003Date of Patent: August 22, 2006Assignee: Syntex (U.S.A.) LLCInventors: Charles Alois Dvorak, Lawrence Emerson Fisher, Keena Lynn Green, Ralph New Harris, III, Hans Maag, Anthony Prince, David Bruce Repke, Russell Stephen Stabler
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Patent number: 7057038Abstract: One aspect of the present invention relates to a method for the kinetic resolution of racemic and diastereomeric mixtures of chiral compounds. The critical elements of the method are: a non-racemic chiral tertiary-amine-containing catalyst; a racemic or diastereomeric mixture of a chiral substrate, e.g., a cyclic carbonate or cyclic carbamate; and a nucleophile, e.g., an alcohol, amine or thiol. A preferred embodiment of the present invention relates to a method for achieving the kinetic resolution of racemic and diastereomeric mixtures of derivatives of ?- and ?-amino, hydroxy, and thio carboxylic acids. In certain embodiments, the methods of the present invention achieve dynamic kinetic resolution of a racemic or diastereomeric mixture of a substrate, i.e.Type: GrantFiled: May 26, 2004Date of Patent: June 6, 2006Assignee: Brandeis UniversityInventors: Li Deng, Jianfeng Hang, Liang Tang
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Patent number: 7053085Abstract: This invention relates to potent selective agonists of the EP4 subtype of prostaglandin E2 receptors, their use or a formulation thereof in the treatment of glaucoma and other conditions, which are related to elevated intraocular pressure in the eye of a patient. This invention further relates to the use of the compounds of this invention for mediating the bone modeling and remodeling processes of the osteoblasts and osteoclasts.Type: GrantFiled: March 10, 2004Date of Patent: May 30, 2006Assignee: Merck & Co. Inc.Inventors: Xavier Billot, John Colucci, Yongxin Han, Marie-Claire Wilson, Robert N. Young
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Patent number: 7038039Abstract: A desired isomer is selectively prepared by phosphorolyzing and isomerizing an anomer mixture of a 1-phosphorylated saccharide derivative while crystallizing one of the isomers to displace the equilibrium. Furthermore, using the action of a nucleoside phosphorylase, a nucleoside is prepared from the 1-phosphorylated saccharide derivative obtained and a base with improved stereoselectivity and a higher yield. This process is an anomer-selective process for preparing a 1-phosphorylated saccharide derivative and a nucleoside.Type: GrantFiled: February 13, 2001Date of Patent: May 2, 2006Assignee: Mitsui Chemicals, Inc.Inventors: Hironori Komatsu, Hirokazu Awano, Nobuyuki Fukazawa, Kiyoshi Ito, Ichirou Ikeda, Tadashi Araki, Takeshi Nakamura, Tamotsu Asano, Junya Fujiwara, Tomoyuki Ando, Katsutoshi Tsuchiya, Kyoko Maruyama, Hideki Umetani, Takahiro Yamauchi, Hitoki Miyake
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Patent number: 6946460Abstract: The invention concerns novel azole or triazole derivatives of formula (I), wherein X, Ar1, Ar2, Ar3, A, B, and R1 are as defined herein, their preparation method and their use as fungicides.Type: GrantFiled: May 2, 2002Date of Patent: September 20, 2005Assignee: Aventis Pharma S.A.Inventors: Didier Babin, John Bernard Weston
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Patent number: 6900161Abstract: The invention concerns novel azole or triazole derivatives of formula (Ia) or (Ib), wherein: X, Ar1, Ar2, Ar3, A, B and R1 are such as defined in the description, the method for preparing same and their use as fungicides.Type: GrantFiled: January 9, 2004Date of Patent: May 31, 2005Assignee: Aventis Pharma S.A.Inventors: Didier Babin, John Bernard Weston
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Patent number: 6858727Abstract: There is disclosed an azetidinone compound of the formula (I): wherein R is hydrogen, or a hydroxy protecting group, R1 and R2 are each independently alkyl of 1-15 carbon atoms, benzyl or cyclized together with the carbon atom to which they are attached to form a 5 or 6-membered cyclic hydrocarbon or a heterocyclic radical having one or two hetero ring atoms, said hetero ring atoms being selected from the group consisting of O and S; R3 is lower alkyl or —COO(lower alkyl) R4 is phenyl, or phenyl substituted with halogen, lower alkoxy or nitro which is useful as a synthetic intermediate to the 1??-methylcarbapenem-type antibacterial agent.Type: GrantFiled: August 6, 2001Date of Patent: February 22, 2005Assignees: Dong Wha Pharm, Ind. Co., Ltd., Korea Research Institute of Chemical TechnologyInventors: Cheol-hae Lee, Bong-jin Kim, Do-kyu Pyun, Won-jang Jeong, Jae-hak Kim, Hee-jung Chung, Hyun-jung Kwak, Eun-jung Kim, Shin-seup Song, Yong-ho Chung
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Patent number: 6841668Abstract: Sterically hindered N-substituted aryloxyamines are prepared by the Keggin polyoxometalate or the transition metal substituted polyoxometalate (TMS-POM) catalyzed decomposition of diazonium salts in the presence of a sterically hindered nitoxyl radical. These compounds are useful as thermal and light stabilizers for a variety of organic substrates.Type: GrantFiled: April 4, 2003Date of Patent: January 11, 2005Assignee: Ciba Specialty Chemicals CorporationInventors: Deborah Judd, Sai P. Shum, Stephen D. Pastor
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Patent number: 6759402Abstract: The present invention relates to novel felbamate derivatives and their use to treat neurological diseases such as epilepsy and to treat tissue damage resulting form ischemic events. The felbamate derivatives are modified to prevent the formation of metabolites that are believed responsible for the toxicity associated with felbamate therapy.Type: GrantFiled: June 6, 2003Date of Patent: July 6, 2004Assignee: University of Virginia Patent FoundationInventors: Timothy L. Macdonald, Thomas A. Miller, Charles D. Thompson, Christine M. Dieckhaus
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Patent number: 6743914Abstract: One aspect of the present invention relates to a method for the kinetic resolution of racemic and diastereomeric mixtures of chiral compounds. The critical elements of the method are: a non-racemic chiral tertiary-amine-containing catalyst; a racemic or diastereomeric mixture of a chiral substrate, e.g., a cyclic carbonate or cyclic carbamate; and a nucleophile, e.g., an alcohol, amine or thiol. A preferred embodiment of the present invention relates to a method for achieving the kinetic resolution of racemic and diastereomeric mixtures of derivatives of &agr;- and &bgr;-amino, hydroxy, and thio carboxylic acids. In certain embodiments, the methods of the present invention achieve dynamic kinetic resolution of a racemic or diastereomeric mixture of a substrate, i.e.Type: GrantFiled: November 20, 2002Date of Patent: June 1, 2004Assignee: Brandeis UniversityInventors: Li Deng, Jianfeng Hang, Liang Tang
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Publication number: 20040087581Abstract: This invention relates to compounds which are generally muscarinic M2/M3 receptor antagonists and which are represented by Formula I: 1Type: ApplicationFiled: October 14, 2003Publication date: May 6, 2004Inventors: Charles Alois Dvorak, Lawrence Emerson Fisher, Keena Lynn Green, Ralph New Harris, Hans Maag, Anthony Prince, David Bruce Repke, Russell Stephen Stabler
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Publication number: 20040002599Abstract: The invention relates to novel substituted benzoylcyclohexenones of the formula (I), 1Type: ApplicationFiled: October 21, 2002Publication date: January 1, 2004Inventors: Klaus-Helmut Muller, Hans-Georg Schwarz, Stefan Herrmann, Dorothee Hoischen, Stefan Lehr, Otto Schallner, Mark Wilhelm Drewes, Peter Dahmen, Dieter Feucht, Rolf Pontzen, Akihiko Yanagi, Shinichi Narabu, Toshio Goto, Seishi Ito, Chieko Ueno
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Patent number: 6664253Abstract: The invention relates to new compounds of formula I or the pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, X and Ar1 have the meanings given in the specification, as well as the preparation and use thereof. The new compounds are valuable neurokinin (tachykinin) antagonists.Type: GrantFiled: October 16, 2001Date of Patent: December 16, 2003Assignee: Boehringer Ingelheim Pharma KGInventors: Horst Dollinger, Franz Esser, Birgit Jung, Gerd Schnorrenberg, Kurt Schromm, Georg Speck
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Patent number: 6562967Abstract: One aspect of the present invention relates to a method for the kinetic resolution of racemic and diastereomeric mixtures of chiral compounds. The critical elements of the method are: a non-racemic chiral tertiary-amine-containing catalyst; a racemic or diastereomeric mixture of a chiral substrate, e.g., a cyclic carbonate or cyclic carbamate; and a nucleophile, e.g., an alcohol, amine or thiol. A preferred embodiment of the present invention relates to a method for achieving the kinetic resolution of racemic and diastereomeric mixtures of derivatives of &agr;- and &bgr;-amino, hydroxy, and thio carboxylic acids. In certain embodiments, the methods of the present invention achieve dynamic kinetic resolution of a racemic or diastereomeric mixture of a substrate, i.e.Type: GrantFiled: November 5, 2001Date of Patent: May 13, 2003Assignee: Brandeis UniversityInventors: Li Deng, Jianfeng Hang, Liang Tang
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Patent number: 6562966Abstract: One aspect of the present invention relates to a method for the kinetic resolution of racemic and diastereomeric mixtures of chiral compounds. The critical elements of the method are: a non-racemic chiral tertiary-amine-containing catalyst; a racemic or diastereomeric mixture of a chiral substrate, e.g., a cyclic carbonate or cyclic carbamate; and a nucleophile, e.g., an alcohol, amine or thiol. A preferred embodiment of the present invention relates to a method for achieving the kinetic resolution of racemic and diastereomeric mixtures of derivatives of &agr;- and &bgr;-amino, hydroxy, and thio carboxylic acids. In certain embodiments, the methods of the present invention achieve dynamic kinetic resolution of a racemic or diastereomeric mixture of a substrate, i.e.Type: GrantFiled: July 31, 2001Date of Patent: May 13, 2003Assignee: Brandeis UniversityInventors: Li Deng, Jianfeng Hang, Liang Tang
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Publication number: 20030087903Abstract: Mevinolin derivatives wherein the lactone ring is modified have interesting pharmaceutical properties, particularly in preventing or treating disorders or diseases mediated by LFA-1/ICAM-1 interactions.Type: ApplicationFiled: July 11, 2002Publication date: May 8, 2003Inventors: Rolf Baenteli, Wilfried Bauer, Sylvain Cottens, Claus Ehrhardt, Ulrich Hommel, Jorg Kallen, Josef Gottfried Meingassner, Francois Nuninger, Gabriele Weitz Schmidt
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Publication number: 20020193314Abstract: A desired isomer is selectively prepared by phosphorolyzing and isomerizing an anomer mixture of a 1-phosphorylated saccharide derivative while crystallizing one of the isomers to displace the equilibrium. Furthermore, using the action of a nucleoside phosphorylase, a nucleoside is prepared from the 1-phosphorylated saccharide derivative obtained and a base with improved stereoselectivity and a higher yield. This process is an anomer-selective process for preparing a 1-phosphorylated saccharide derivative and a nucleoside.Type: ApplicationFiled: May 7, 2002Publication date: December 19, 2002Inventors: Hironori Komatsu, Hirokazu Awano, Nobuyuki Fukazawa, Kiyoshi Ito, Ichirou Ikeda, Tadashi Araki, Takeshi Nakamura, Tamotsu Asano, Junya Fujiwara, Tomoyuki Ando, Katsutoshi Tsuchiya, Kyoko Maruyama, Hideki Umetani, Takahiro Yamauchi, Hitoki Miyake
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Publication number: 20020165390Abstract: The invention relates to a process for preparing quinoline-substituted carbonate and carbamate compounds, which are important intermediates in the synthesis of 6-O-substituted macrolide antibiotics. The process employs metal-catalyzed coupling reactions to provide a carbonate or carbamate of formula (I) or (II) or a substrate that can be reduced to obtain the same.Type: ApplicationFiled: April 29, 2002Publication date: November 7, 2002Inventors: Michael S. Allen, Ramiya H. Premchandran, Sou-Jen Chang, Stephen Condon, John A. DeMattei, Steven A. King, Lawrence Kolaczkowski, Sukumar Manna, Paul J. Nichols, Hemant H. Patel, Subhash R. Patel, Daniel J. Plata, Eric J. Stoner, Jien-Heh J. Tien, Steven J. Wittenberger
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Patent number: 6472529Abstract: A compound of the formula: is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.Type: GrantFiled: April 18, 2001Date of Patent: October 29, 2002Assignee: Abbott LaboratoriesInventors: Hing Leung Sham, Daniel W. Norbeck, Xiaoqi Chen, David A. Betebenner, Dale J. Kempf, Thomas R. Herrin, Gondi N. Kumar, Stephen L. Condon, Arthur J. Cooper, Daniel A. Dickman, Steven M. Hannick, Lawrence Kolaczkowski, Patricia A. Oliver, Daniel J. Plata, Peter J. Stengel, Eric J. Stoner, Jieh-Heh J. Tien, Jih-Hua Liu, Ketan M. Patel
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Patent number: 6469000Abstract: Disclosed are compounds which are inhibitors of metalloproteases having the following structure: where Ar, W, X, Y, Z, R1 and R2 have the meanings described in the specification and optical isomers, diastereomers, and enantiomers thereof or a pharmaceutically-acceptable salt, or biohydrolyzable amides, esters, or imides thereof. Also disclosed are pharmaceutical compositions and methods of treating diseases, disorders and conditions characterized by unwanted metalloprotease activity using these compounds or pharmaceutical compositions.Type: GrantFiled: August 29, 2000Date of Patent: October 22, 2002Assignee: The Procter & Gamble Co.Inventors: Stanislaw Pikul, Kelly Lynn McDow-Dunham, Neil Gregory Almstead, Biswanath De, Michael George Natchus, Yetunde Olabisi Taiwo
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Patent number: 6407232Abstract: The invention relates an ionic metal complex represented by the general formula (1): wherein M is an element of groups 3-15 of the periodic table; Aa+ represents a metal ion, onium ion or proton; X1 represents O, S or NR5R6; each of R1 and R2 independently represents H, a halogen, a C1-C10 alkyl group or C1-C10 halogenated alkyl group; R3 represents a C1-C10 alkylene group, C1-C10 halogenated alkylene group, C4-C20 aryl group or C4-C20 halogenated aryl group; R4 represents a halogen, C1-C10 alkyl group, C1-C10 halogenated alkyl group, C4-C20 aryl group, C4-C20 halogenated aryl group or X2R7; X2 represents O, S or NR5R6; each of R5 and R6 represents H or a C1-C10 alkyl group; and R7 represents a C1-C10 alkyl group, C1-C10 halogenated alkyl group, C4-C20 aryl group or C4-C20 halogenated aryl group. The ionic metal complex can be used as a supporting electrolyte for electrochemical devices, a polymerization catalyst of polyolefins and so forth, or a catalyst for organic synthesis.Type: GrantFiled: July 25, 2000Date of Patent: June 18, 2002Assignee: Central Glass Company, LimitedInventors: Shoichi Tsujioka, Hironari Takase, Mikihiro Takahashi
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Patent number: 6365587Abstract: The present application describes novel substituted aryl hydroxamic acids of formula I: or pharmaceutically acceptable salt forms thereof, wherein ring A is a 5-8 membered ring containing from 0-1 additional heteroatoms selected from N, O, and S, which are useful as metalloprotease inhibitors.Type: GrantFiled: May 13, 1999Date of Patent: April 2, 2002Inventors: Matthew E. Voss, Carl P. Decicco, Ruth R. Wexler
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Publication number: 20020037895Abstract: Mevinolin derivatives wherein the lactone ring is modified have interesting pharmaceutical properties, particularly in preventing or treating disorders or diseases mediated by LFA-1/ICAM-1 interactions.Type: ApplicationFiled: August 13, 2001Publication date: March 28, 2002Inventors: Rolf Baenteli, Wilfried Bauer, Sylvain Cottens, Claus Ehrhardt, Ulrich Hommel, Joerg Kallen, Josef Gottfried Meingassner, Francois Nuninger, Gabriele Weitz Schmidt
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Patent number: 6355796Abstract: An improved process and intermediate compounds for the preparation of 2-(N,N-disubstituted)amino-4-(perfluoroalkyl)-1,3-oxazin-6-one compounds having the structural formula I and an improved process for the preparation of 6-(perfluoroalkyl)uracil compounds having the structural formula VType: GrantFiled: February 3, 2000Date of Patent: March 12, 2002Assignee: BASF AktiengesellschaftInventor: Venkataraman Kameswaran
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Patent number: 6340751Abstract: Disclosed is a process for the preparation of a 4-substituted azetidinone derivative, which comprises reacting an azetidinone derivative and an amide compound in the presence of a magnesium compound such as those represented by the following formulas (II): and (IV): represented by the following formula (III): MgR5R6 (III) wherein R5 represents a C1-12 alkyl group, a C2-5 alkenyl group, a 5- to 8-membered alicyclic group which may be substituted by a lower C1-4 alkyl group, a phenyl group which may be substituted by a lower C1-4 alkyl group, a lower C1-4 alkoxy group or a halogen atom or a benzyl group which may be substituted by a lower C1-4 alkyl group, a lower C1-4 alkoxy group or a halogen atom, and R6 represents a halogen atom, a methanesulfonyloxy group, a benzenesulfonyloxy group, a p-toluenesulfonyloxy group, a trifluoromethanesulfonyloxy group, an acetoxy group which may be substituted by a halogen atom or a cyano group or an OR7 group (R7 representingType: GrantFiled: July 19, 1999Date of Patent: January 22, 2002Assignee: Takasago International CorporationInventors: Takao Saito, Toshiyuki Murayama, Takaji Matsumoto, Takashi Miura
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Publication number: 20020004503Abstract: A compound of the formula: 1Type: ApplicationFiled: April 18, 2001Publication date: January 10, 2002Inventors: Hing Leung Sham, Daniel W. Norbeck, Xiaoqi Chen, David A. Betebenner, Dale J. Kempf, Thomas R. Herrin, Gondi N. Kumar, Stephen L. Condon, Arthur J. Cooper, Daniel A. Dickman, Steven M. Hannick, Lawrence Kolaczkowski, Patricia A. Oliver, Daniel J. Plata, Peter J. Stengel, Eric J. Stoner, Jieh-Heh J. Tien, Jih-Hua Liu, Ketan M. Patel
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Patent number: 6265400Abstract: The present invention relates generally to cyclic carbamates and isoxazolidines or Formula (I) or their pharmaceutically acceptable salts thereof, which are useful as antagonists of the platelet glycoprotein IIb/IIIa fibrinogen receptor complex, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds for the inhibition of platelet aggregation, as thrombolytics, and/or for the treatment of thromboembolic disorders.Type: GrantFiled: June 28, 1999Date of Patent: July 24, 2001Assignee: Dupont Pharmaceuticals CompanyInventors: Fuqiang Jin, Pasquale Nicholas Confalone
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Patent number: 6251897Abstract: A 6-phenyltetrahydro-1,3-oxazin-2-one derivative having the formula (I): wherein, R1 is an unsubstituted or substituted C1 to C8 alkyl group; an unsubstituted or substituted C3 to C7 cycloalkyl group;, etc., R2 is a C1 to C4 alkyl group, R3 is H; an unsubstituted or substituted C1 to C5 alkyl group; etc., R4 is H; an unsubstituted or substituted C1 to C6 alkyl group, and R5 and R6 are independently a hydrogen atom; an unsubstituted or substituted C1 to C5 alkyl group; etc. an optical isomer thereof, or a pharmacologically acceptable salt thereof, or a hydrate or a solvate thereof and pharmaceutical compositions containing the same, in particular a drug for the prevention or treatment of inflammatory diseases and a drug for asthma. The above 6-phenyltetrahydro-1,3-oxazin-2-one derivative has a strong type IV PDE inhibitory activity and has a bronchiodilator and antiinflammatory effects.Type: GrantFiled: February 1, 1999Date of Patent: June 26, 2001Assignee: Nikken Chemicals Co., LTDInventors: Shinji Ina, Kenjirou Yamana, Kyoji Noda
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Patent number: 6235901Abstract: A novel compound having the formula: wherein R is an alkyl group containing 1-5 carbon atoms or an aryl, substituted aryl, substituted or unsubstituted heteroaryl, alkyl-aryl, alkylether-aryl or O; R1 and R2 are hydrogen or a methyl group; X is O, NH, NR′ wherein R′ is an alkyl group containing 1-5 carbon atoms, or O—R″ or NR″ wherein O—R″ is O-alkyl-O or O-alkyl, NR″ is O-alkyl-ONH, wherein each instance alkyl contains 1-5 carbon atoms and n is 0 or 1. The compound of this invention is useful as a monomer which can be polymerized and/or copolymerized by catonic polymerization. Polymers and copolymers produced in this invention can be crosslinked and are useful in coatings, inks, overprint varnishes, and surface treatment applications.Type: GrantFiled: May 6, 1999Date of Patent: May 22, 2001Assignee: S. C. Johnson Commercial Markets, Inc.Inventors: Bill M. Culbertson, David L. Trumbo
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Patent number: 6166010Abstract: The invention relates to the use of azine derivatives, some of which are known, of the formula ##STR1## in which A represents substituted phenyl, or represents in each case optionally substituted naphthyl, pyridyl, thienyl or pyrazolyl;B represents hydrogen, alkyl or in each case optionally substituted phenyl, phenylalkyl, phenylalkenyl, phenoxyalkyl, phenylthioalkyl, phenylsulfinylalkyl or phenylsulfonylalkyl;D represents hydrogen or alkyl;E represents hydrogen, alkyl or in each case optionally substituted phenyl, phenylalkyl, phenoxyalkyl, phenylthioalkyl, phenylsulfinylalkyl or phenylsulfonylalkyl;G represents hydrogen or alkyl;J represents hydrogen or alkyl;K represents hydrogen, alkyl or optionally substituted phenyl; orB and D or D and G or E and G together represent optionally substituted alkanediyl, wherein one or two CH.sub.2 groups are optionally replaced by O and/or S; andW and Y are different and represent N, O or S, wherein the ring always contains an N atom,for combating animal pests.Type: GrantFiled: July 14, 1994Date of Patent: December 26, 2000Assignees: Yashima Chemical Industry Co., LTD, Bayer AktiengesellschaftInventors: Yoshiaki Itoh, Tatsuya Ishida, Yasuo Kikuchi, Junji Suzuki, Chiharu Morikawa, Yokichi Tsukidate, Kichizo Kudoh, Graham Holmwood, Udo Kraatz, Ulrike Wachendorff-Neumann, Christoph Erdelen
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Patent number: 6159902Abstract: The invention relates to 1,3-oxazin-4-one derivatives of formula (I): ##STR1## and to their use as herbicides.Type: GrantFiled: June 10, 1998Date of Patent: December 12, 2000Assignees: Mitsubishi Chemical Corporation, Rhone-Poulenc Agriculture LTDInventors: Tetsuya Murata, Hideshi Mukaida, Yoshie Yamada, Yukiko Oe, Norishige Toshima, Sachio Kudo, Kouichi Araki, Atsushi Go, Masahito Ito, Virginia Smith, Thomas Yarwood, Michael Gingell, Lyn Jennens
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Patent number: 6080857Abstract: A method for the preparation of .beta.-amino acid compounds is provided. The method includes contacting an amine nucleophile with an .alpha.,.beta.-unsaturated amide compound in the presence of a chiral Lewis acid complex. The chiral Lewis acid complex is formed from an azophilic metal salt and a chiral bisoxazolinylmethane compound. The selective amidolysis of one enantiomer of the .beta.-aminoamide product is also described.Type: GrantFiled: February 13, 1998Date of Patent: June 27, 2000Assignee: North Dakota State UniversityInventors: Mukund Prahalada Rao Sibi, John Joseph Shay, Craig Peter Jasperse, Mei Liu
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Patent number: 6046135Abstract: 1,3-Oxazin-4-one derivatives of formula (I): ##STR1## wherein Q represents --C(.dbd.O)--, --CH(OH)-- or --C(OR.sup.11)(OR.sup.11)--, in which R.sup.11 represents lower alkyl; or the two groups --OR.sup.11, together with the carbon atom to which they are attached, form a five or six membered cyclic ketal group; and their use as herbicides.Type: GrantFiled: September 2, 1998Date of Patent: April 4, 2000Assignees: Rhone-Poulenc Agriculture Ltd, Mitsubishi Chemical CorporationInventors: Michael Colin Cramp, Yoshihiro Usui, Sachio Kudo