Three Or More Ring Hetero Atoms In The Bicyclo Ring System Patents (Class 544/48)
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Patent number: 6096771Abstract: An isoxazole compound having the following formula: ##STR1## wherein R.sup.1 represents hydrogen, halogen, alkyl, alkoxy, hydroxyl, alkylthio, amino, alkanoyl, alkanoylamino, alkanoyloxy, alkoxycarbonyl, carboxy, (alkylthio)thiocarbonyl, carbamoyl, nitro or cyano; R.sup.2 represents an amino; m is 2 or 3; n is 1 to 6; ring A represents a phenyl ring, a naphthyl ring or an aromatic heterocycle; and X represents oxygen or sulfur. The isoxazole compound has an excellent monoamine oxidase inhibitory activity, and is useful for treating Parkinson's disease, depression and Alzheimer's disease.Type: GrantFiled: February 3, 1999Date of Patent: August 1, 2000Assignee: Sankyo Company, LimitedInventors: Koichi Kojima, Junichi Sakai, Yuichi Aizawa, Naozumi Samata, Masao Kozuka, Kenji Yoshimi, Isao Kaneko, Kazuo Koyama
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Patent number: 6093710Abstract: A compound of the formula ##STR1## in which R.sup.1 is hydrogen, lower alkyl, optionally substituted ar(lower)alkyl, cyclo(lower)alkyl(lower)alkyl, protected carboxy)lower)alkyl, carboxy)lower)alkyl, hydroxy(lower)alkyl, optionally substituted lower alkylcarbamoyl(lower)alkyl, lower alkylthio(lower)alkyl, carboxy(lower)alkanoyl, protected carboxy(lower)alkanoyl, aroyl, lower alkanoyl, or optionally substituted arylcarbamoyl(lower)alkyl,R.sup.2 is hydrogen, carboxy, protected carboxy, formyl or N-(lower)alkyl-N-(lower)alkoxycarbamoyl,R.sup.3 is hydrogen or amidino-protective group,A is lower alkylene or carbonyl,X is ##STR2## Y is --S-- or --SO.sub.2 --, Z is --S-- or --O--,or pharmaceutically acceptable salts thereofwhich is useful as a medicament.Type: GrantFiled: March 12, 1999Date of Patent: July 25, 2000Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Akito Tanaka, Hiroaki Mizuno, Minoru Sakurai
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Patent number: 6083515Abstract: Nonsteroidal antiinflammatory drugs which have been substituted with a nitrogen monoxide group; compositions comprising (i) a nonsteroidal antiinflammatory drug, which can optionally be substituted with a nitrogen monoxide group and (ii) a compound that directly donates, transfers or releases a nitrogen monoxide group (preferably as a charged species, particularly nitrosonium); and methods of treatment of inflammation, pain, gastrointestinal lesions and/or fever using the compositions are disclosed. The compounds and compositions protect against the gastrointestinal, renal and other toxicities that are otherwise induced by nonsteroidal antiinflammatory drugs.Type: GrantFiled: January 22, 1999Date of Patent: July 4, 2000Assignee: NitroMed, Inc.Inventors: David S. Garvey, L. Gordon Letts, H. Burt Renfroe, Sang William Tam
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Patent number: 6071860Abstract: Compounds of the formula (I) and salts thereof ##STR1## where R.sup.1 to R.sup.5, A, Z, X, X', n and m are as defined in claim 1 are suitable as herbicides and plant growth regulators.Type: GrantFiled: February 6, 1997Date of Patent: June 6, 2000Assignee: Hoechst Schering AgrEvo GmbHInventors: Wolfgang Giencke, Lothar Willms, Klaus Bauer, Hermann Bieringer, Christopher Rosinger
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Patent number: 6069114Abstract: Compounds of the formula (I) and their salts ##STR1## in which R.sup.1 to R.sup.6, Y.sup.1, to Y.sup.2, Y.sup.3, m and n are as defined in claim 1 are suitable as herbicides and plant growth regulators. They can be prepared analogously to known processes using intermediates of the formula (V) (cf. claim 6).Type: GrantFiled: February 25, 1997Date of Patent: May 30, 2000Assignee: Hoechst Schering AgrEvo GmbHInventors: Klaus Lorenz, Klemens Minn, Lothar Willms, Klaus Bauer, Hermann Bieringer, Christopher Rosinger
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Patent number: 6046211Abstract: The current invention discloses useful pharmaceutical compositions containing amidino derivative useful as nitric oxide synthase inhibitors.Type: GrantFiled: May 6, 1998Date of Patent: April 4, 2000Assignee: G.D. Searle & Co.Inventors: Donald W. Hansen, Jr., Mark G. Currie, E. Ann Hallinan, Kam F. Fok, Timothy J. Hagen, Arija A. Bergmanis, Steven W. Kramer, Len F. Lee, Suzanne Metz, William M. Moore, Karen B. Peterson, Barnett S. Pitzele, Dale P. Spangler, R. Keith Webber, Mihaly V. Toth, Mahima Trivedi, Foe S. Tjoeng
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Patent number: 6037469Abstract: Compounds of formula (I) in which: R.sup.1 is hydrogen or an organic substituent group; R.sup.2 is a fused bicyclic heterocyclic ring system of general formula (a) wherein R.sup.4 and R.sup.5 are independently hydrogen or one or more substituents replacing hydrogen atoms in the ring system shown; m is 2 or 3; p is 0, 1 or 2; and R.sup.3 is hydrogen, a salt-forming cation or an ester-forming group; and the symbol .dbd./.dbd.Type: GrantFiled: May 24, 1995Date of Patent: March 14, 2000Assignee: SmithKline Beecham plcInventors: Nigel John Perryman Broom, Frank Peter Harrington
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Patent number: 6004954Abstract: This invention relates to a compound of the following formula or a salt thereof, their production and use. ##STR1## wherein R.sup.1 and R.sup.2 independently represent hydrogen, a group bonding through a carbon atom, a group bonding through a nitrogen atom, a group bonding through an oxygen atom, or a group bonding through a sulfur atom; R.sup.3 represents hydrogen, halogen, a group bonding through a carbon atom, a group bonding through a nitrogen atom, a group bonding through an oxygen atom, or a group bonding through a sulfur atom; W represents an oxygen atom or sulfur atom; A represents a group forming a nitrogen-containing condensed ring at the 3,4- of a 1,4-thiazine ring; R.sup.1 and R.sup.2 may be combined to form a bivalent hydrocarbon group interrupted by one or more hetero atoms or an alkylene group.Type: GrantFiled: March 10, 1997Date of Patent: December 21, 1999Assignee: Takeda Chemical Industries, Ltd.Inventors: Shuichi Furuya, Seiichi Tanida, Yoshikazu Ohta
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Patent number: 5998408Abstract: The compounds of Formula I ##STR1## are useful as immunosuppressive agents.Type: GrantFiled: October 8, 1997Date of Patent: December 7, 1999Assignee: Merck & Co., Inc.Inventors: Robert K. Baker, Frank Kayser, Jianming Bao, Andrew Kotliar, William H. Parsons, Kathleen M. Rupprecht
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Patent number: 5990145Abstract: The present invention relates to compounds of the formula I,A--B--D--E--F--G (I)in which A, B, D, E, F and G have the meanings given in the patent claims, to their preparation and to their use as medicaments. The compounds of the invention are used as vitronectin receptor antagonists and as inhibitors of bone resorption.Type: GrantFiled: December 22, 1997Date of Patent: November 23, 1999Assignees: Hoechst Aktiengesellschaft, Genentech, Inc.Inventors: Volkmar Wehner, Hans Ulrich Stilz, Anuschirwan Peyman, Karlheinz Scheunemann, Jean-Marie Ruxer, Denis Carniato, Jean-Michel Lefrancois, Thomas Richard Gadek, Robert McDowell
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Patent number: 5981748Abstract: The invention relates to methods of making compounds of the formula VII ##STR1## and their enantiomers, where Ar is a substituted or unsubstituted five- or six-membered aromatic group and B is either an amino acid linked through the amino portion to form an amide or a C.sub.1 -C.sub.6 alcohol linked through the alcohol portion to form an ester. These compounds are advantageously employed as intermediates to prepare optically pure compounds that are active GARFT inhibitors. In one method, a compound of the formula ##STR2## is reacted with a compound of the formula ##STR3## where X is a halogen.Type: GrantFiled: July 2, 1998Date of Patent: November 9, 1999Assignee: Agouron Pharmaceuticals, Inc.Inventors: Michael D. Varney, William H. Romines, Cynthia L. Palmer
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Patent number: 5972975Abstract: Substituted 2-aminopyridine compounds of Formula (I) and pharmaceutically acceptable salts which have been found useful in the treatment of nitric oxide synthase mediated diseases and disorders.Type: GrantFiled: May 22, 1997Date of Patent: October 26, 1999Assignee: Merck & Co., Inc.Inventors: Craig Esser, William Hagmann, William Hoffman, Shrenik Shah, Kenny Wong, Renee Chabin, Ravindra Guthikonda, Malcolm Maccoss, Charles Caldwell, Philippe Durette
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Patent number: 5889002Abstract: 1,2,4-Thiadiazine and 1,4-thiazine derivatives represented by the formula ##STR1## wherein A, B, D, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are defined in the description, compositions thereof and methods for preparing the compounds are described. The compounds are useful in the treatment of diseases of the central nervous system, the cardiovascular system, the pulmonary system, the gastrointestinal system and the endocrinologic system.Type: GrantFiled: January 17, 1997Date of Patent: March 30, 1999Assignee: Novo Nordisk A/SInventors: Flemming Elmelund Nielsen, Holger Claus Hansen, John Bondo Hansen, Tina M.o slashed.ller Tagmose
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Patent number: 5852159Abstract: The present invention relates to plastics comprising a high molecular weight, sterically hindered amine, wherein the sterically hindered amine is at least one amine from the group consisting ofI: oligomerized 2,2,4,4-tetramethyl-20(oxiranylmethyl)-7-oxa-3,20-diazadispiro?5.1.11.2!he neicosan-21-one,II: condensation product of 2-chloro-4,6-di(4-n-butylamino-1,2,2,6,6-pentamethylpiperidyl)-1,3,5-triaz ine and 1,2-bis(3-aminopropylamino)ethane, andIII: condensation product of 1-hydroxyethyl-2,2,6,6-tetramethyl-4-hydroxypiperidine and succinic acid.These plastics exhibit a reduced rate of uptake of sulfur compounds.The invention further relates to shaped articles made from these plastics.Type: GrantFiled: May 10, 1996Date of Patent: December 22, 1998Assignee: Hoechst AktiengesellschaftInventors: Matthias Zah, Gerhard Pfahler, Karl Gaa, Klaus Keck-Antoine
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Patent number: 5846970Abstract: This invention is directed to bicyclic pyrimidine derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-states characterized by thrombotic activity.Type: GrantFiled: June 17, 1997Date of Patent: December 8, 1998Assignee: Berlex Laboratories, Inc.Inventors: Brad O. Buckman, Raju Mohan, Michael M. Morrissey
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Patent number: 5792764Abstract: Pyrido-1,2,4-thiadiazine and pyrido-1,4-thiazine derivatives represented by the formula ##STR1## wherein A, B, D, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are defined in the description, compositions thereof and methods for preparing the compounds are described. The compounds are useful in the treatment of diseases of the central nervous system, the cardiovascular system, pulmonary system, the gastrointestinal system and the endocrinologic system.Type: GrantFiled: January 17, 1997Date of Patent: August 11, 1998Assignee: Novo Nordisk A/SInventors: Bernard Pirotte, Philippe Lebrun, Pascal De Tullio, Fabian Somers, Jacques Delarge, Holger Claus Hansen, Flemming Elmelund Nielsen, John Bondo Hansen
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Patent number: 5789587Abstract: There are disclosed certain novel compounds identified as heterocyclic-fused lactams which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. Growth promoting compositions containing such heterocyclic-fused lactams as the active ingredient thereof are also disclosed.Type: GrantFiled: November 6, 1996Date of Patent: August 4, 1998Assignee: Merck & Co., Inc.Inventors: Michael H. Fisher, Helmut Mrozik, William R. Schoen, Thomas L. Shih, Matthew J. Wyvratt
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Patent number: 5703073Abstract: Nonsteroidal antiinflammatory drugs which have been substituted with a nitrogen monoxide group; compositions comprising (i) a nonsteroidal antiinflammatory drug, which can optionally be substituted with a nitrogen monoxide group and (ii) a compound that directly donates, transfers or releases a nitrogen monoxide group (preferably as a charged species, particularly nitrosonium); and methods of treatment of inflammation, pain, gastrointestinal lesions and/or fever using the compositions are disclosed. The compounds and compositions protect against the gastrointestinal, renal and other toxicities that are otherwise induced by nonsteroidal antiinflammatory drugs.Type: GrantFiled: October 13, 1995Date of Patent: December 30, 1997Assignee: NitroMed, Inc.Inventors: David S. Garvey, L. Gordon Letts, H. Burt Renfroe, Sang William Tam
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Patent number: 5703058Abstract: A method and composition for the treatment of HIV and HBV infections in humans and other host animals is disclosed that includes the administration of an effective amount of a ?5-carboxamido or 5-fluoro!-2',3'-dideoxy-2',3'-didehydro-pyrimidine nucleoside or a ?5-carboxamido or 5-fluoro!-3'-modified-pyrimidine nucleoside, or a mixture or a pharmaceutically acceptable derivative thereof, including a 5' or N.sup.4 alkylated or acylated derivative, or a pharmaceutically acceptable salt thereof, in a pharmaceutically acceptable carrier.Type: GrantFiled: January 27, 1995Date of Patent: December 30, 1997Assignee: Emory UniversityInventors: Raymond F. Schinazi, Dennis C. Liotta
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Patent number: 5698553Abstract: A benzylpiperidine compound of formula I ##STR1## in which R.sup.1 is H, Hal or nitro,R.sup.2 is a benzyl group, which is unsubstituted or substituted by Hal on the aromatic portion, in the 2-, 3- or 4-position of the piperidine ring, with the proviso that R.sup.2 is not in the 4-position if X is --CO--, Y and Z are --CH.sub.2 and R.sup.1 is H,R.sup.3 is H or A,X is --O--, --S--, --NH--, --CO-- or --SO.sub.2 --,Y is --CH.sub.2 --, --NH--, --O--, --S--, --NH-- or alternatively --CO-- if X is --CO-- and Z is --NH-- or --NA--,Z is --CH.sub.2 --, --C(A).sub.2-, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, --CO--, --NH--, --NA--, --O--, --S-- or a bond,wherein X--Y or Y--Z is not --O--, --S--S--, --NH--O--, --O--NH--, --NH--NH--, --O--S-- or --S--O,A is alkyl having 1-6 C atoms,B is O or both H and OH, i.e.Type: GrantFiled: October 30, 1995Date of Patent: December 16, 1997Assignee: Merck Patent Gesellschaft Mit Beschrankter HaftungInventors: Helmut Prucher, Rudolf Gottschlich, Joachim Leibrock, Harry Schwartz
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Patent number: 5693641Abstract: This invention is directed to bicyclic pyrimidine derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-states characterized by thrombotic activity.Type: GrantFiled: August 16, 1996Date of Patent: December 2, 1997Assignee: Berlex Laboratories Inc.Inventors: Brad O. Buckman, Raju Mohan, Michael M. Morrissey
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Patent number: 5679678Abstract: Thienothiazine derivatives of the formula ##STR1## are provided. These derivatives are useful for the treatment of inflammation and pain.Type: GrantFiled: December 14, 1994Date of Patent: October 21, 1997Assignee: Chemisch Pharmazeutische Forschungsgesellschaft m.b.H.Inventors: Dieter Binder, Josef Weinberger, Michael Pyerin
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Patent number: 5677300Abstract: A pyridothiazineacetic acid compound of the formula (I) ##STR1## wherein each symbol is as defined in the specification, a pharmaceutically acceptable salt thereof, production thereof, and a pharmaceutical composition, an aldose reductase inhibitor and a preparation for the prevention and treatment of the complications of diabetes, containing the same.The pyridothiazineacetic acid compound and a pharmaceutically acceptable salt thereof of the present invention have an aldose reductase inhibitory action and are superior in safety. Accordingly, they are useful as a preparation for the prevention and treatment of the complications of diabetes, such as faulty union of corneal injury, cataract, neurosis, retinopathy and nephropathy, particularly, cataract and neurosis. In addition, the production method of the present invention enables efficient production of said pyridothiazineacetic acid compound.Type: GrantFiled: September 3, 1996Date of Patent: October 14, 1997Assignees: The Green Cross Corporation, Senji Pharmaceutical Co., Ltd.Inventors: Hiroshi Hosono, Tomoji Aotsuka, Yoshiyuki Nakamura, Tetsuo Matsui, Hiromichi Ishikawa
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Patent number: 5672599Abstract: Compounds of the formula ##STR1## wherein X is O or S--(O).sub.t ; n is one; m is zero or one; Y is CH.sub.2, O, or S--(O).sub.t provided that Y is O or S--(O).sub.t only when m is one; and A is ##STR2## are dual inhibitors of NEP and ACE. Compounds wherein A is ##STR3## are selective ACE inhibitors. Also disclosed are methods of preparation and intermediates.Type: GrantFiled: November 22, 1995Date of Patent: September 30, 1997Assignee: Bristol-Myers Squibb Co.Inventor: Jeffrey A. Robl
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Patent number: 5668278Type: GrantFiled: July 31, 1996Date of Patent: September 16, 1997Assignee: Hoeschst Schering AgrEvo GmbHInventors: Uwe Hartfiel, Gabriele Dorfmeister, Helga Franke, Jens Geisler, Gerhard Johann, Richard Rees
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Patent number: 5646141Abstract: Compounds of the Formula I, which are in equilibrium with their 4-hydroxy tautomers and are in the form of diastereomeric mixtures, and their pharmaceutically acceptable salts are potent GARFT inhibitors: ##STR1## In the above formula, A is S, CH.sub.2 or Se, and Z, X, R.sub.1 and R.sub.2 are as defined in the specification. These compounds and their salts are useful as antiproliferative agents. The invention also pertains to pharmaceutical compositions and methods employing such compounds as GARFT inhibitors or antiproliferative agents.Type: GrantFiled: June 6, 1995Date of Patent: July 8, 1997Assignee: Agouron Pharmaceuticals, Inc.Inventors: Michael D. Varney, William H. Romines
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Patent number: 5646142Abstract: New thiophene sulfonamides useful as carbonic anhydrase inhibitors are disclosed. Methods for using the compounds to control IOP are also disclosed.Type: GrantFiled: July 8, 1994Date of Patent: July 8, 1997Assignee: Alcon Laboratories, Inc.Inventors: Anura P. Dantanarayana, Thomas R. Dean, Jesse A. May
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Patent number: 5643855Abstract: Compounds such as Formula I having herbicidal utility are disclosed: ##STR1## wherein Q is ##STR2## R.sub.1 is H; alkyl, haloalkyl or halogen R.sup.2 is C.sub.1 -C.sub.2 alkyl optionally substituted with one or more halogens, OR.sup.8, CN, COR.sup.9, CO.sub.2 R.sup.31 or CONR.sup.32 R.sup.33 ; CN; CO.sub.2 R.sup.34 ; CONR.sup.35 R.sup.36 ; S(O).sub.n R.sup.8 ; S(O).sub.n NR.sup.19 R.sup.8 or COR.sup.37 ; orR.sup.1 and R.sup.2 can be taken together along with the carbon to which they are attached to form C.dbd.CHCO.sub.2 R.sup.31 ; C.dbd.(CH.sub.3)CO.sub.2 R.sup.31 ; C.dbd.(C.sub.2 H.sub.5)CO.sub.2 R.sup.31 ; C.dbd.CHCONR.sup.32 R.sup.33 ; C.dbd.C(CH.sub.3)CONR.sup.32 R.sup.33 or C.dbd.C(C.sub.2 H.sub.5)CONR.sup.32 R.sup.33.Type: GrantFiled: June 15, 1995Date of Patent: July 1, 1997Assignee: E. I. Du Pont de Nemours and CompanyInventor: John Jolly Kilama
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Patent number: 5641774Abstract: The invention generally relates to compounds of the formula I, which are in equilibrium with their 4-hydroxy tautomers, and their pharmaceutically acceptable salts: ##STR1## where n is 0 to 2; A is S, CH.sub.2, O, NH or Se, and when n is 0, A is not CH.sub.2, and when n is 1, A is not CH.sub.2 or NH; X is a substituted or unsubstituted C.sub.1 --C.sub.3 alkyl, C.sub.2 -C.sub.3 alkenyl, C.sub.2 -C.sub.3 alkynyl or amino, or sulfur or oxygen; Ar is a substituted or unsubstituted monocyclic carbocycle or heterocycle, or fused or nonfused polycyclic carbocycle or heterocycle; and R.sub.1 and R.sub.2 are hydrogen or a moiety that forms together with the attached CO.sub.2 a readily hydrolyzable ester group. These compounds and their salts are useful as inhibitors of GARFT or as antiproliferative agents. The invention also pertains to pharmaceutical compositions and methods employing such compounds as GARFT inhibitors or antiproliferative agents.Type: GrantFiled: June 7, 1995Date of Patent: June 24, 1997Assignee: Agouron Pharmaceuticals, Inc.Inventors: Michael D. Varney, William H. Romines, Cynthia L. Palmer
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Patent number: 5641771Abstract: The invention generally relates to compounds of the formula I, which are in equilibrium with their 4-hydroxy tautomers, and their pharmaceutically acceptable salts: ##STR1## where n is 0 to 2; A is S, CH.sub.2, O, NH or Se, and when n is 0, A is not CH.sub.2, and when n is 1, A is not CH.sub.2 or NH; X is a substituted or unsubstituted C.sub.1 -C.sub.3 alkyl, C.sub.2 -C.sub.3 alkenyl, C.sub.2 -C.sub.3 alkynyl or amino, or sulfur or oxygen; Ar is a substituted or unsubstituted monocyclic carbocycle or heterocycle, or fused or nonfused polycyclic carbocycle or heterocycle; and R.sub.1 and R.sub.2 are hydrogen or a moiety that forms together with the attached CO.sub.2 a readily hydrolyzable ester group. These compounds and their salts are useful as inhibitors of GARFT or as antiproliferative agents. The invention also pertains to pharmaceutical compositions and methods employing such compounds as GARFT inhibitors or antiproliferative agents.Type: GrantFiled: June 7, 1995Date of Patent: June 24, 1997Assignee: Agouron Pharmaceuticals, Inc.Inventors: Michael D. Varney, William H. Romines, Cynthia L. Palmer
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Patent number: 5639749Abstract: The invention generally relates to compounds of the formula I, which are in equilibrium with their 4-hydroxy tautomers, and their pharmaceutically acceptable salts: ##STR1## where n is 0 to 2; A is S, CH.sub.2, O, NH or Se, and when n is 0, A is not CH.sub.2, and when n is 1, A is not CH.sub.2 or NH; X is a substituted or unsubstituted C.sub.1 -C.sub.3 alkyl, C.sub.2 -C.sub.3 alkenyl, C.sub.2 -C.sub.3 alkynyl or amino, or sulfur or oxygen; Ar is a substituted or unsubstituted monocyclic carbocycle or heterocycle, or fused or nonfused polycyclic carbocycle or heterocycle; and R.sub.1 and R.sub.2 are hydrogen or a moiety that forms together with the attached CO.sub.2 a readily hydrolyzable ester group. These compounds and their salts are useful as inhibitors of GARFT or as antiproliferative agents. The invention also pertains to pharmaceutical compositions and methods employing such Compounds as GARFT inhibitors or antiproliferative agents.Type: GrantFiled: June 7, 1995Date of Patent: June 17, 1997Assignee: Agouron Pharmaceuticals, Inc.Inventors: Michael D. Varney, William H. Romines, Cynthia L. Palmer
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Patent number: 5639747Abstract: The invention generally relates to compounds of the formula I, which are in equilibrium with their 4-hydroxy tautomers, and their pharmaceutically acceptable salts: ##STR1## where n is 0 to 2; A is S, CH.sub.2, O, NH or Se, and when n is 0, A is not CH.sub.2, and when n is 1, A is not CH.sub.2 or NH; X is a substituted or unsubstituted C.sub.1 -C.sub.3 alkyl, C.sub.2 -C.sub.3 alkenyl, C.sub.2 -C.sub.3 alkynyl or amino, or sulfur or oxygen; Ar is a substituted or unsubstituted monocyclic carbocycle or heterocycle, or fused or nonfused polycyclic carbocycle or heterocycle; and R.sub.1 and R.sub.2 are hydrogen or a moiety that forms together with the attached CO.sub.2 a readily hydrolyzable ester group. These compounds and their salts are useful as inhibitors of GARFT or as antiproliferative agents. The invention also pertains to pharmaceutical compositions and methods employing such compounds as GARFT inhibitors or antiproliferative agents.Type: GrantFiled: June 7, 1995Date of Patent: June 17, 1997Assignee: Agouron Pharmaceuticals, Inc.Inventors: Michael D. Varney, William H. Romines, Cynthia L. Palmer
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Patent number: 5629423Abstract: A process for synthesizing enantiomerically pure chiral secondary alcohol compounds linked to a heterocyclic core moiety, using a natural chiral molecule starting material. The inventive process is particularly useful for bulk manufacturing of chiral secondary alcohol compounds.Type: GrantFiled: May 23, 1995Date of Patent: May 13, 1997Assignee: Cell Therapeutics, Inc.Inventors: J. Peter Klein, Alistair J. Leigh, John Michnick, Anil M. Kumar, Gail E. Underiner
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Patent number: 5625061Abstract: Compounds of the invention include those of the following formula: ##STR1## In this formula, A is oxygen, sulfur or selenium; X' is a substituted or unsubstituted C.sub.1 -C.sub.3 alkyl group, a substituted or unsubstituted C.sub.2 -C.sub.3 alkenyl group, a substituted or unsubstituted C.sub.2 -C.sub.3 alkynyl group, a substituted or unsubstituted amino group, sulfur or oxygen; Y is oxygen, sulfur or NH; B is hydrogen or a halogen; C is hydrogen, a halogen or a substituted or unsubstituted C.sub.1 -C.sub.6 alkyl group; and R.sub.6 is hydrogen or a moiety that forms with the attached CO.sub.2 a readily hydrolyzable ester group.Type: GrantFiled: June 7, 1995Date of Patent: April 29, 1997Assignee: Agouron Pharmaceuticals, Inc.Inventors: Michael D. Varney, William H. Romines, Cynthia L. Palmer
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Patent number: 5610318Abstract: This invention is directed to a process for preparing a compound containing a persalt activators and salts thereof which are derived from imidocarboxylic acids and sulfimidocarboxylic acids of the formula I: ##STR1## in which A is a group of the formula ##STR2## n is the number 0, 1 or 2, R.sup.1 is hydrogen, chlorine, bromine, C.sub.1 -C.sub.20 -alkyl, C.sub.2 -C.sub.20 -alkenyl, aryl, or alkylaryl,R.sup.2 is hydrogen, chlorine, bromine, --SO.sub.3 M, --CO.sub.2 M or --OSO.sub.3 M, X is C.sub.1 -C.sub.19 -alkylene or arylene,B is a group of the formula C.dbd.O or SO.sub.2,L is a leaving group.Type: GrantFiled: May 31, 1995Date of Patent: March 11, 1997Assignee: Hoechst AktiengesellschaftInventors: Frank Jaekel, Gerd Reinhardt, Wolf-Dieter M uller
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Patent number: 5594139Abstract: The invention generally relates to compounds of the formula I, which are in equilibrium with their 4-hydroxy tautomers, and their pharmaceutically acceptable salts: ##STR1## where n is 0 to 2; A is S, CH.sub.2, O, NH or Se, and when n is 0, A is not CH.sub.2, and when n is 1, A is not CH.sub.2 or NH; X is a substituted or unsubstituted C.sub.1 -C.sub.3 alkyl, C.sub.2 -C.sub.3 alkenyl, C.sub.2 -C.sub.3 alkynyl or amino, or sulfur or oxygen; Ar is a substituted or unsubstituted monocyclic carbocycle or heterocycle, or fused or nonfused polycyclic carbocycle or heterocycle; and R.sub.1 and R.sub.2 are hydrogen or a moiety that forms together with the attached CO.sub.2 a readily hydrolyzable ester group. These compounds and their salts are useful as inhibitors of GARFT or as antiproliferative agents. The invention also pertains to pharmaceutical compositions and methods employing such compounds as GARFT inhibitors or antiproliferative agents.Type: GrantFiled: July 28, 1994Date of Patent: January 14, 1997Assignee: Agouron Pharmaceuticals, Inc.Inventors: Michael D. Varney, William H. Romines, Cynthia L. Palmer
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Patent number: 5585377Abstract: Sulfonamides and pharmaceutical compositions containing the compounds useful in controlling intraocular pressure are disclosed. Methods for controlling intraocular pressure through administration of the compositions are also disclosed.Type: GrantFiled: December 23, 1994Date of Patent: December 17, 1996Assignee: Alcon Laboratories, Inc.Inventors: Thomas R. Dean, Jesse A. May, Hwang-Hsing Chen
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Patent number: 5571773Abstract: There are provided novel (2-imidazolin-2-yl) fused heteropyridine compounds, and intermediate compounds for the preparation thereof, and a method for controlling a wide variety of annual and perennial plant species therewith.Type: GrantFiled: June 2, 1995Date of Patent: November 5, 1996Assignee: American Cyanamid CompanyInventors: Barrington Cross, Marinus Los, Robert F. Doehner, Jr., David W. Ladner, Jerry L. Johnson
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Patent number: 5538966Abstract: Compounds of the following formula are disclosed:Compounds of Formula I are the topic of this invention: ##STR1## Wherein G, J and the two atoms of the thiophene ring to which they are attached form a six-membered ring chosen from ##STR2## The compounds are useful as carbonic anhydrase inhibitors.Type: GrantFiled: January 20, 1995Date of Patent: July 23, 1996Assignee: Alcon Laboratories, Inc.Inventors: Jesse A. May, Hwang-Hsing Chen, Brian DuPr e, Thomas R. Dean
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Patent number: 5534483Abstract: There are provided novel (2-imidazolin-2-yl) fused heteropyridine compounds, and intermediate compounds for the preparation thereof, and a method for controlling a wide variety of annual and perennial plant species therewith.Type: GrantFiled: June 2, 1995Date of Patent: July 9, 1996Assignee: American Cyanamid CompanyInventors: Barrington Cross, Marinus Los, Robert F. Doehner, Jr., David W. Ladner, Jerry L. Johnson
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Patent number: 5527796Abstract: Thienothiazine derivatives of the formula ##STR1## in which X denotes a single bond, a straight chain or branched carbon chain having 1-12 C-atoms in the chain, it being possible for this chain to contain one or more double or triple bonds and/or two or more heteroatoms, Y denotes a single bond, and R denotes a monocyclic or polycyclic, optionally partly hydrogenated aryl, heteroaryl, arlyoxy, arylaza, heteroarylaza, arylthio or heteroarylthio radical which can optionally be substituted by lower alkyl, mono- or poyhalogenated lower alkyl, perfluorinated lower alkyl, alkoxy or halogen, and their use.Type: GrantFiled: February 18, 1994Date of Patent: June 18, 1996Assignee: Chemisch Pharmazeutische Forschungsgesellschaft m.b.H.Inventors: Dieter Binder, Josef Weinberger
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Patent number: 5508272Abstract: Compounds of the formula ##STR1## wherein X is O or S--(O).sub.t ; n is one or two; m is zero or one; Y is CH.sub.2, O, or S--(O).sub.t provided that Y is O or S--(O).sub.t only when m is one; and A is ##STR2## are dual inhibitors of NEP and ACE. Compounds wherein A is ##STR3## are selective ACE inhibitors. Also disclosed are methods of preparation and intermediates.Type: GrantFiled: May 5, 1994Date of Patent: April 16, 1996Assignee: Bristol-Myers Squibb CompanyInventor: Jeffrey A. Robl
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Patent number: 5504095Abstract: Aminobenzosultam derivatives, which are inhibitors of lipoxygenase, having the formula ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein Ar is cycloalkyl having five to seven carbon atoms, tetrahydropyranyl, pyridyl, oxazolyl, phenyl or substituted phenyl wherein said substituent is methyl, methoxy, fluoro, chloro or trifluoromethyl; n is an integer of 1 to 3; X is hydrogen, methyl, methoxy, fluoro, chloro or trifluoromethyl; Z is --NH--, --O--, or --CH.sub.2 --; and R.sup.1 is hydrogen or alkyl having one to three carbon atoms.Type: GrantFiled: December 20, 1994Date of Patent: April 2, 1996Assignee: Pfizer Inc.Inventors: Masami Nakane, Kunio Satake, Kazuo Ando, Hiroaki Wakabayashi
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Patent number: 5475105Abstract: Abstract of the Disclosure: Compounds of the formula I ##STR1## where R.sup.1, R.sup.2, n , R.sup.3, A, X, Y and Z have the meanings stated in the description, and the preparation thereof are described. The novel compounds are suitable for controlling diseases , i.e., as neuroleptics, antidepressants, sedatives, hypnotics, CNS protectives or muscle relaxants.Type: GrantFiled: December 16, 1994Date of Patent: December 12, 1995Assignee: BASF AktiengesellschaftInventors: Gerd Steiner, Liiane Unger, Berthold Behl, Hans-Juergen Teschendorf, Rainer Munschauer
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Patent number: 5472960Abstract: Nitro-substituted heterocyclic compounds of the formula (I) ##STR1## wherein R is hydrogen or alkyl,Z is an optionally substituted aryl or optionally substituted heterocyclic group containing at least one atom selected from N, O and S,A is optionally substituted ethylene or optionally substituted trimethylene, andB stands for 2 or 3 members of a heterocyclic ring which is formed, together with the adjacent C-atom and N-atom and at least one of said members may represent a hetero atom and may be optionally substituted, provided that when B stands for 3 members, two of which are carbon atoms and the other one is a nitrogen atom which is located in the middle of the three members, then at least one of said two carbon atoms must be substituted by a keto group. Such compounds being useful as insecticides.Type: GrantFiled: August 16, 1994Date of Patent: December 5, 1995Assignee: Nihon Bayer Agrochem K.K.Inventors: Kozo Shiokawa, Shinichi Tsuboi, Shoko Sasaki, Koichi Moriya, Yumi Hattori, Katsuhiko Shibuya
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Patent number: 5473067Abstract: A process for synthesizing carbonic anhydrase inhibitors is disclosed.Type: GrantFiled: January 14, 1994Date of Patent: December 5, 1995Assignee: Alcon Laboratories, Inc.Inventors: William D. Dean, Paul W. Zinke, Steven J. Sproull, Michael E. Deason, Raymond E. Conrow, Anura P. Dantanarayana
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Patent number: 5470973Abstract: Enantioselective syntheses of (S)-6-chloro-3,4-dihydro-2-(3-methoxypropyl)-2H-thieno[3,2-e]-1,2-thiazin- 4-ol 1,1-dioxide and related compounds are described.Type: GrantFiled: October 3, 1994Date of Patent: November 28, 1995Assignee: Alcon Laboratories, Inc.Inventor: Roman Hoff
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Patent number: 5463056Abstract: Thiophene derivatives of formula (I) ##STR1## wherein X and Y are the same or different O, S or N--R.sup.3,Z is a C.sub.1 -C.sub.6 -alkylene residue that may be substituted by R.sup.1 and R.sup.2,R.sup.1, R.sup.2 are the same or different hydrogen, or --(CH.sub.2).sub.n --OR.sup.4, --CH.dbd.CH.sub.2 or ##STR2## n is 1 to 10, R.sup.3 is aryl, C.sub.1-18 -alkyl or H,R.sup.4 is SO.sub.3.sup.- (H.sup.+,Na.sup.+,K.sup.+,Li.sup.+) or --(CH.sub.2 --CH.sub.2 --O).sub.m --R.sup.5,m is 1 to 10 andR.sup.5 is alkyl with 1 to 6 C atoms,wherein compounds in which X and Y are both O and R.sup.1 and R.sup.2 are both hydrogen atoms are excluded, are suitable for the preparation of polythiophenes which can be used as organic electrical conductors.Type: GrantFiled: May 27, 1994Date of Patent: October 31, 1995Assignee: Agta-Gevaerf AGInventor: Friedrich Jonas
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Patent number: 5444066Abstract: The present invention provides a thioformamide derivative represented by the following general formula (I) or a pharmacologically acceptable salt thereof, which is highly safe, easy to use, and useful as an excellent hypotensive or heart disease remedy: ##STR1## wherein Y represents ##STR2## or the like [wherein R.sup.7 represents benzyloxy or the like; R.sup.11 and R.sup.12 each represent hydrogen, hydroxyl, benzoyloxy, benzyloxy, ##STR3## (wherein R.sup.14 and R.sup.15 each represent hydrogen, benzyl or the like) or the like];Z represents --CH.sub.2 -- or the like; A represents imidazolyl or imidazopyridyl which may have one or two substituents, or the like; R.sup.1 and R.sup.2 each represent hydrogen, lower alkyl or the like; and R.sup.3 and R.sup.4 each represent hydrogen, lower alkyl or the like.Type: GrantFiled: April 26, 1994Date of Patent: August 22, 1995Assignee: Eisai Co., Ltd.Inventors: Yasuhiro Kabasawa, Fumihiro Ozaki, Keiji Ishibashi, Takashi Hasegawa, Hitoshi Oinuma, Toshiaki Ogawa, Hideyuki Adachi, Hiroshi Katoh, Kohtarou Kodama, Hideto Ohara, Nobuyuki Mori, Norio Minami
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Patent number: 5405829Type: GrantFiled: June 13, 1994Date of Patent: April 11, 1995Assignee: Schering AktiengesellschaftInventors: Uwe Hartfiel, Gabriele Dorfmeister, Helga Franke, Jens Geisler, Gerhard Johann, Richard Rees