Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To Ring Carbon Of The Oxazole Ring By Nonionic Bonding Patents (Class 548/248)
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Patent number: 6083986Abstract: Compounds useful as potassium channel inhibitors and especially useful for the treatment of cardiac arrhythmias and cell proliferative disorders are described.Type: GrantFiled: July 15, 1997Date of Patent: July 4, 2000Assignees: ICAgen, Inc., Eli Lilly & CompanyInventors: Neil Alexander Castle, Sean Patrick Hollinshead, Philip Floyd Hughes, Jose Serafin Mendoza, Joseph Wendell Wilson, George Salvatore Amato, Serge Beaudoin, Michael Gross, Grant McNaughton-Smith
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Patent number: 6075026Abstract: Disclosed are compounds of formula I: or the pharmaceutically acceptable salts thereof whereinX is a carbonyl, sulfonyl, methylene, or methylene substituted with optionally substituted phenyl;Z is nitrogen or CH;Ar.sub.1 and Ar.sub.2 independently represent aryl groups; andY is hydrogen; orY and R.sub.1 or R.sub.2 together represent CH.sub.2 ;CH.sub.2 CH.sub.2 ; CH.sub.2 O; CH.sub.2 S forming a five or six membered ring and such ring may be optionally substituted with loweralkyl or phenyl; or pharmaceutically acceptable salts thereof, useful in the treatment of neoplastic diseases, and bacterial or fungal infections, and for preventing or decreasing the production of abnormally phosphorylated paired helical filament (PHF) epitopes associated with Alzheimer's Disease and, therefore for treating Alzheimer's Disease.Type: GrantFiled: April 21, 1997Date of Patent: June 13, 2000Assignee: Molecular Geriatrics, Corp.Inventors: John Francis DeBernardis, Daniel Joseph Kerkman, Raymond Paul Zinkowski
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Patent number: 6069115Abstract: The invention relates to a method for the control of weeds at a crop locus, said method comprising the application of an effective amount of:(a) a glyphosate herbicide which is glyphosate or a derivative thereof; and(b) at least one HPPD-inhibiting herbicide;wherein the crop is tolerant to glyphosate and optionally the HPPD-inhibiting herbicide.Type: GrantFiled: November 12, 1997Date of Patent: May 30, 2000Assignee: Rhone-Poulenc AgrochimieInventors: Ken Pallett, Richard Derose, Bernard Pelissier, Alain Sailland, Thomas Edward Vrabel
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Patent number: 6060494Abstract: The invention relates to a crystal modification of the compound of the formula I ##STR1## and the processes for the preparation of and use that crystal modifications 1. The invention is used for treating acute immunological episodes, such as sepsis, allergies, graft-versus-host and host-versus-graft-reactions, autoimmune diseases, in particular rheumatoid arthritis, systemic lupus erythematosus, multiple sclerosis, psoriasis, atopic dermatitis, asthma, urticaria, rhinitis, uveitis, type II diabetes, liver fibrosis, cystic fibrosis, colitis, cancers, such as lung cancer, leukemia, ovarian cancer, sarcomas, Kaposi's sarcoma, meningioma, intestinal cancer, lymphatic cancer, brain tumors, breast cancer, pancreatic cancer, prostate cancer, or skin cancer.Type: GrantFiled: August 6, 1998Date of Patent: May 9, 2000Assignee: Hoechst Marion Roussel Deutschland GmbHInventors: Holger Faasch, Udo Hedtmann, Uwe Westenfelder, Erich Paulus
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Patent number: 6037312Abstract: Isoxazole derivatives of the formula (I), ##STR1## and herbicides containing the above isoxazole derivatives as active ingredients, which can selectively control grass weeds and broad-leaved weeds simultaneously at a low dosage as a single herbicide, without causing phytotoxicity on corn, sorgo, cotton, wheat and barley.Type: GrantFiled: February 3, 1999Date of Patent: March 14, 2000Assignee: Idemitsu Kosan Co., Ltd.Inventors: Yoriyuki Takashima, Hideki Kamano, Masashi Sakamoto
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Patent number: 6022868Abstract: Disclosed are compounds of formula (I) selected from the following ##STR1## wherein Y is ##STR2## and wherein A, B, C, D, R, k, m, n, o, p, s, t and u are as defined in the specification. These compounds are useful in treating diseases in the central nervous system related to malfunctioning of the nicotinic cholinergic system.Type: GrantFiled: December 19, 1997Date of Patent: February 8, 2000Assignee: Novo Nordisk AlsInventors: Preben Houlberg Olesen, John Bondo Hansen
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Patent number: 6020371Abstract: Picornaviral 3C protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the picornaviral 3C protease. These compounds, as well as pharmaceutical compositions that contain these compounds, are suitable for treating patients or hosts infected with one or more picornaviruses.Type: GrantFiled: December 16, 1997Date of Patent: February 1, 2000Assignee: Agouron Pharmaceuticals, Inc.Inventors: Peter S. Dragovich, Thomas J. Prins, Ru Zhou
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Patent number: 6013805Abstract: The invention relates to intermediates to herbicidal compounds of formulae (Ia), (Ib) or (Ic): ##STR1##Type: GrantFiled: September 29, 1998Date of Patent: January 11, 2000Assignee: Rhone-Poulenc Agriculture LtdInventor: David William Hawkins
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Patent number: 5998613Abstract: The present invention relates to novel 4-aminotetrahydrobenzisoxazoles or 4-aminotetrahydrobenziothiazoles having gamma-aminobutanoic acid (GABA)-uptake inhibiting activity and thus useful in the treatment of analgesia, psychosis, convulsions, anxiety, epileptic disorders or muscular and movement disorders, such as spastic disorders or symptoms in Huntington's disease or Parkinson disease.Type: GrantFiled: August 5, 1997Date of Patent: December 7, 1999Assignee: H. Lundbeck A/SInventors: Erik Falch, Jens Kristian Perregaard, Arne Schousboe, Povl Krogsgaard-Larsen, Bente Frolund, Sibylle Moltzen Lenz
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Patent number: 5985799Abstract: Compounds of Formula (I), and their N-oxides and agriculturally-suitable salts, are disclosed which are useful in controlling undesired vegetation, wherein J is Formula (II), Q is represented by Q-1 through Q-4 and X, Y, Z, R.sup.1-19, m, n, p, q, and r are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula (I) and a method for controlling undesired vegetation which involves contacting the vegetation or its environment with an effective amount of a compound of Formula (I).Type: GrantFiled: May 12, 1998Date of Patent: November 16, 1999Assignee: E.I. du Pont de Nemours and CompanyInventor: Chi-Ping Tseng
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Patent number: 5977149Abstract: Cyclic amides of Formula (I) which are useful as fungicides wherein: A is O; S; N; NR.sup.5 ;or CR.sup.14--, G is C or N; W is O or S; X is OR.sup.1, S(O).sub.m R.sup.1 or halogen; R.sup.1, R.sup.2, and R.sup.5 are independently, in part, C.sub.1 -C.sub.6 alkyl; Y is, in part, --O--; --S(O).sub.n --,--CHR.sup.6 O--; or --CHR.sup.6 O--N.dbd.C(R.sup.7)--; Z is, in part, optionally substituted cycloalkyl, phenyl, pyridinyl, pyrimidinyl, or naphthyl; and R.sup.3, R.sup.4, R.sup.6, R.sup.7, R.sup.14, m, and n are defined in the disclosure, are disclosed.Type: GrantFiled: January 14, 1998Date of Patent: November 2, 1999Assignee: E. I. du Pont de Nemours and CompanyInventors: Richard James Brown, King-Mo Sun, Deborah Ann Frasier
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Patent number: 5977151Abstract: A compound of the formula ##STR1## where R.sup.1 is the radical of the formula II or III ##STR2## is suitable for the production of a pharmaceutical for the treatment of inflammations, carcinomatous diseases, or autoimmune diseases. A compound of the formula IV ##STR3## is suitable for the production of specific antibodies against a compound of the formula I for the discovery of specific-binding proteins from cell extracts, serum, blood, or synovial fluids, for the purification of proteins, for the modification of microtiter plates, or for the preparation of chromatography material, in particular of affinity chromatography material, and for use in diagnostics.Type: GrantFiled: January 23, 1998Date of Patent: November 2, 1999Assignee: Hoechst AktiengesellschaftInventors: Stefan Mullner, Bernd Kirschbaum, Wilfried Schwab
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Patent number: 5965740Abstract: A compound represented by the formula (I): ##STR1## wherein R.sup.1 is an optionally substituted heterocyclic group; R.sup.2 is optionally substituted aryl or heterocyclic group; R.sup.3 is hydrogen, alkyl, alkenyl, or alkynyl; R.sup.4 is hydrogen, alkyl, alkoxy, halogen, nitro, cyano, or halogenated alkyl; M is oxygen, S(O).sub.i wherein i is 0, 1, or 2, NR.sup.5 wherein R.sup.5 is hydrogen, alkyl, or acyl, --Q--N.dbd.C(R.sup.6)--, --B--C(R.sup.8).dbd.N--, --CH.dbd.N--N.dbd.C(R.sup.9)--, or --CH.dbd.N--A--(CR.sup.10 R.sup.11)m--; and n is 0, 1, or 2, an intermediate for producing the same and an agrochemical composition containing the same as an active ingredient.Type: GrantFiled: February 20, 1998Date of Patent: October 12, 1999Assignee: Shionogi & Co., Ltd.Inventors: Hiroyuki Kai, Akira Takase, Toshikazu Ohtsuka
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Patent number: 5962487Abstract: Picornaviral 3C protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of picornaviral 3C proteases. These compounds, as well as pharmaceutical compositions that contain these compounds, are suitable for treating patients or hosts infected with one or more picornaviruses. Several novel methods and intermediates can be used to prepare the novel picornaviral 3C protease inhibitors of the present invention.Type: GrantFiled: December 16, 1997Date of Patent: October 5, 1999Assignee: Agouron Pharmaceuticals, Inc.Inventors: Stephen E. Webber, Peter S. Dragovich, Thomas J. Prins, Ethel S. Littlefield, Joseph T. Marakovits, Robert E. Babine
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Patent number: 5935973Abstract: Compounds of formula I ##STR1## and pharmaceutically acceptable salts thereof in which A is methylene or O; B is methylene or O; g is 0,1,2,3 or 4; R.sub.1 is an optional substituent; U is an alkylene chain optionally substituted by one or more alkyl; Q represents a divalent group containing nitrogen atoms; and T represents CO.HET, have utility in the treatment of central nervous system disorders, for example depression, anxiety, psychoses (for example schizophrenia), tardive dyskinesia, Parkinson's disease, obesity, hypertension, Tourette's syndrome, sexual dysfunction, drug addiction, drug abuse, cognitive disorders, Alzheimer's disease, senile dementia, obsessive-compulsive behavior, panic attacks, social phobias, eating disorders and anorexia, cardiovascular and cerebrovascular disorders, non-insulin dependent diabetes mellitus, hyperglycaemia, constipation, arrhythmia, disorders of the neuroendocrine system, stress, prostatic hypertrophy, and spasticity.Type: GrantFiled: January 5, 1998Date of Patent: August 10, 1999Assignee: Knoll AktiengesellschaftInventors: Alan Martin Birch, David John Heal, Frank Kerrigan, Keith Frank Martin, Patricia Lesley Needham, Bruce Jeremy Sargent
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Patent number: 5885983Abstract: Compounds are provided which inhibit microsomal triglyceride transfer protein and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases. The compounds have the structure ##STR1## wherein R.sup.1 to R.sup.6, Q, and X are as defined herein.Type: GrantFiled: April 23, 1997Date of Patent: March 23, 1999Assignee: Bristol-Myers Squibb CompanyInventors: Scott A. Biller, John K. Dickson, Jr.
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Patent number: 5859257Abstract: A class of substituted isoxazolyl compounds is described for use in treating cyclooxygenase-2 related disorders. Compounds of particular interest are defined by Formula I ##STR1## wherein R.sup.1, R.sup.2, and R.sup.3, are described in the specification.Type: GrantFiled: August 14, 1996Date of Patent: January 12, 1999Assignee: G. D. Searle & Co.Inventor: John J Talley
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Patent number: 5856274Abstract: The invention relates to 4-benzoylisoxazoles having the formula: ##STR1## wherein: R is hydrogen or --CO.sub.2 R.sup.5 ;R.sup.1 is alkyl, cyclopropyl or 1-methylcyclopropyl;R.sup.2 is chlorine, bromine, optionally substituted alkyl, alkoxy, haloalkoxy, --S(O).sub.p R.sup.61, nitro or cyano;R.sup.3 is --S(O).sub.n R.sup.6 ;R.sup.4 is hydrogen, fluorine, chlorine, bromine, optionally substituted alkyl, alkoxy, S(O).sub.q R.sup.61, nitro, cyano or --CO.sub.2 R.sup.52 ;R.sup.5 and R.sup.61, which are the same or different, are each alkyl or haloalkyl;R.sup.52 is alkyl;R.sup.6 is alkyl, alkenyl or alkynyl optionally substituted by one or more halogen; andn, p and q, which are the same or different, are each zero, one or two;and their use as herbicides.Type: GrantFiled: September 14, 1995Date of Patent: January 5, 1999Assignee: Rhone-Poulenc Agriculture LimitedInventors: Susan Mary Cramp, Claude Lambert, Derek Ian Wallis, Thomas Yarwood
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Patent number: 5849928Abstract: The invention relates to compounds of formulae (Ia), (Ib) or (Ic): ##STR1## and to their use as herbicides.Type: GrantFiled: March 21, 1997Date of Patent: December 15, 1998Assignee: Rhone-Poulenc Agriculture LimitedInventor: David William Hawkins
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Patent number: 5849736Abstract: This invention relates to novel isoxazolines and isoxazoles which are useful as antagonists of the platelet glycoprotein IIb/IIIa fibrinogen receptor complex or the vitronectin receptor, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of platelet aggregation, as thrombolytics, and/or for the treatment of thromboembolic disorders.Type: GrantFiled: May 31, 1995Date of Patent: December 15, 1998Assignee: The DuPont Merck Pharmaceutical CompanyInventors: John Wityak, Chu-Biao Xue, Thais Motria Sielecki-Dzurdz, Richard Eric Olson, William Frank Degrado, Gary Avonn Cain, Douglas Guy Batt, Donald Pinto, Munir Alwan Hussain, Shaker Ahmed Mousa
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Patent number: 5834468Abstract: This invention relates to substituted and unsubstituted ???(aryl- and heteroaryl-) alkyl-, alkyloxy-, alkylthio-, oxo-, thio-, and alkylamino!- heteroaryl and aryl!- alkylamino-, aminoalkyl-, alkyloxy-, and alkylthio!- aryl and heteroaryl compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof, which are useful as antagonists of the pain enhancing effects of E-type prostaglandins, to processes for the preparation of such compounds, to pharmaceutical compositions comprising such compounds, and to methods for treating pain comprising the administration of such compounds.Type: GrantFiled: July 2, 1996Date of Patent: November 10, 1998Assignee: Zeneca LimitedInventors: Gloria Anne Breault, John Oldfield, Howard Tucker, Peter Warner
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Patent number: 5814627Abstract: A compound having the formula (I), a physiologically tolerable salt of the compound having the formula (I) and/or a steroisomeric form of the compound having the formula (I), in which one residue R.sup.1 or R.sup.2 stands for the formula (II), are suitable for preparing medicaments for the therapy of inflammations, asthma, rheumatoid diseases and auto-immune diseases.Type: GrantFiled: November 19, 1996Date of Patent: September 29, 1998Assignee: Hoechst AktienegesellschaftInventors: Wilfried Schwab, Hiristo Anagnostopulos, Robert Ryder Bartlett, Rudolf Schleyerbach, Klaus Ulrich Weithmann
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Patent number: 5780393Abstract: There are provided isoxazole- and isothiazole-5-carboxamide compounds of formula I ##STR1## which are useful for the control of undesirable monocotyledenous and dicotyledenous plant species in the presence of crops such as cereal and leguminous crops. Also provided are herbicidal compositions and methods of using same.Type: GrantFiled: August 23, 1996Date of Patent: July 14, 1998Assignee: American Cyanamid CompanyInventor: Trevor W. Newton
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Patent number: 5760066Abstract: Compounds and methods for inhibiting hyper-proliferative cell growth. The compounds and method are preferably used to treat patients having a hyper-proliferative cell disorder.Type: GrantFiled: April 19, 1996Date of Patent: June 2, 1998Assignee: Sugen, Inc.Inventor: Peng Cho Tang
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Patent number: 5760244Abstract: A process for the preparation of 3-isoxazolecarboxlic acid which is an intermediate for prepearing useful compounds is provided, said process being characterized in that a compound of formula (I) is reacted with hydroxylamine to obtain a compound of formula (II), and the compound thus obtained is treated with an alkali: ##STR1## wherein R.sup.1 is a lower alkyl, R.sup.2 is a carboxy protecting group, X is a halogen atom, and Y is a hydrogen atom, or X and Y together may form a single bond.Type: GrantFiled: July 28, 1997Date of Patent: June 2, 1998Assignee: Shionogi & Co., Ltd.Inventors: Susumu Takada, Nobuo Chomei, Masaaki Uenaka
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Patent number: 5750543Abstract: A compound having the structure: ##STR1## wherein (a) n is from 1 to about 3;(b) X is selected from the group consisting of O, S, SO, or SO.sub.2 ;(c) Y is independently hydrogen or straight, branched or cyclic alkyl having from 1 to about 4 carbon atoms, or the Y's are bonded together to form an alkanyl ring having from about 3 to about 7 atoms;(d) Z is hydrogen or straight, branched or cyclic alkyl having from 3 to about 10 atoms other than hydrogen;(e) W is O or S; and(f) Het is a heteroaryl group comprising one or more rings each ring containing from about 5 to about 6 atoms other than hydrogen and wherein the group contains at least one heteroatom selected from O, N, or S.pharmaceutical compositions comprising such compounds, and methods of treating inflammation or pain using such compounds.Type: GrantFiled: February 1, 1996Date of Patent: May 12, 1998Assignee: The Procter & Gamble CompanyInventors: Laurence Ichih Wu, John Michael Janusz
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Patent number: 5747424Abstract: The invention relates to 4-substituted isoxazole derivatives of formula I: ##STR1## wherein R, R.sup.1, R.sup.2, Q and n have the meanings defined in the description, which possess valuable herbicidal properties.Type: GrantFiled: May 1, 1997Date of Patent: May 5, 1998Assignee: Rhone-Poulenc Agriculture Ltd.Inventors: David Alan Roberts, Susan Mary Cramp, Derek Ian Wallis, Jean-Paul Bulot
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Patent number: 5741801Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof, and the use of a compound of formula (I) or a pharmaceutically acceptable salt thereof:X--CO--CH.sub.2 --Z (I)whereinX is a monocyclic or polycyclic aromatic group,Z is of sub-formula (h), (j) or (k): ##STR1## wherein n.sup.1 is 1, 2, 3 or 4; n.sup.2 is 0, 1, 2, 3 or 4; n.sup.3 is 2, 3, 4 or 5;q is 0, 1, 2 or 3; p is 0, 1 or 2; m is 0, 1 or 2;R.sub.5 is hydrogen, C.sub.1-12 alkyl, aralkyl or R.sub.5 is (CH.sub.2).sub.z --R.sub.10 wherein z is 2 or 3 and R.sub.10 is selected from cyano, hydroxyl, C.sub.1-6 alkoxy, phenoxy, C(O)C.sub.1-6 alkyl, COC.sub.6 H.sub.5, --CONR.sub.11 R.sub.12, NR.sub.11 COR.sub.12, SO.sub.2 NR.sub.11 R.sub.12 or NR.sub.11 SO.sub.2 R.sub.12 wherein R.sub.11 and R.sub.12 are hydrogen or C.sub.1-6 alkyl; or R.sub.Type: GrantFiled: November 22, 1995Date of Patent: April 21, 1998Assignee: SmithKline Beecham plcInventors: Francis David King, Laramie Mary Gaster, Keith Raymond Mulholland
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Patent number: 5703017Abstract: 3-(Het)arylcarboxylic acid derivatives of the formula I ##STR1## where R is formyl, CO.sub.2 H or a radical hydrolyzable to COOH and the other substituents have the following meanings:R.sup.2 and R.sup.3 are each halogen, alkyl, haloalkyl, alkoxy, haloalkoxy or alkylthio;X is nitrogen or CR.sup.14, where R.sup.14 is hydrogen or, together with R.sup.3, forms an alkylene or alkenylene chain, in each of which a methylene group is replaced by oxygen;R.sup.4 is phenyl or naphthyl, each of which is unsubstituted or substituted or an unsubstituted or substituted five-membered or six-membered heteroaromatic structure containing one to three nitrogen atoms or one sulfur or oxygen atom;R.sup.5 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, haloalkyl, alkoxyalkyl, alkylthioalkyl or phenyl;R.sup.6 is C.sub.1 -C.sub.8 -alkyl, C.sub.3 -C.sub.6 -alkenyl, C.sub.3 -C.sub.6 -alkynyl or C.sub.3 -C.sub.Type: GrantFiled: October 19, 1995Date of Patent: December 30, 1997Assignee: BASF AktiengesellschaftInventors: Ernst Baumann, Joachim Rheinheimer, Uwe Josef Vogelbacher, Matthias Bratz, Hans Theobald, Matthias Gerber, Karl-Otto Westphalen, Helmut Walter, Wilhelm Rademacher
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Patent number: 5696271Abstract: A process for the preparation of 3-isoxazolecarboxlic acid which is an intermediate for prepearing useful compounds is provided, said process being characterized in that a compound of formula (I) is reacted with hydroxylamine to obtain a compound of formula (II), and the compound thus obtained is treated with an alkali: ##STR1## wherein R.sup.1 is a lower alkyl, R.sup.2 is a carboxy protecting group, X is a halogen atom, and Y is a hydrogen atom, or X and Y together may form a single bond.Type: GrantFiled: August 7, 1996Date of Patent: December 9, 1997Assignee: Shionogi & Co., Ltd.Inventors: Susumu Takada, Nobuo Chomei, Masaaki Uenaka
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Patent number: 5693804Abstract: Disclosed are compounds of formula I: ##STR1## wherein X is a carbonyl, sulfonyl, methylene, or methylene substituted with optionally substituted phenyl;Z is nitrogen or CH;Ar.sub.1 and Ar.sub.2 independently represent aryl groups; andY is hydrogen; orY and R.sub.1 or R.sub.2 together represent CH.sub.2 ;CH.sub.2 CH.sub.2 ; CH.sub.2 O; CH.sub.2 S forming a five or six membered ring and such ring may be optionally substituted with loweralkyl or phenyl; or the pharmaceutically acceptable salts thereof, useful in the treatment of neoplastic diseases, and bacterial or fungal infections, and in preventing or decreasing the production of abnormally phosphorylated paired helical filament (PHF) epitopes associated with Alzheimer's Disease and, therefore, useful for treating Alzheimer's Disease.Type: GrantFiled: November 17, 1994Date of Patent: December 2, 1997Assignee: Molecular Geriatrics CorporationInventors: John Francis DeBernardis, Daniel Joseph Kerkman, Raymond Paul Zinkowski
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Patent number: 5691366Abstract: A new nitro compound of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are each lower alkyl or lower alkoxy(lower)-alkyl, or ##STR2## is cyclized to form ##STR3## X is --O--, --S-- or --NH--, m is an integer 0 or 1, andR.sup.3 is carbamoyl, lower alkylcarbamoyl, lower alkanoyl, di-lower alkylaminosulfonyl, lower alkylsulfonyl, oxamoyl or a group of the formula: --(Y).sub.n --R.sup.4 wherein Y is --CO--, --SO.sub.2 --, --COCH.sub.2 -- or ##STR4## n is an integer of 0 or 1, and R.sup.4 is heterocyclic group which is optionally substituted with one or more substituents selected from lower alkyl, lower alkoxy, phenyl, carbamoyl, halogen, amino, lower alkylthio, hydroxy, lower alkylsulfonylamino and carbamoylmethyl, and pharmaceutically acceptable salt thereof, which are useful as vasodilators.Type: GrantFiled: October 31, 1995Date of Patent: November 25, 1997Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Masayuki Kato, Shigetaka Nishino, Mitsuko Hamano, Hisashi Takasugi
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Patent number: 5670656Abstract: A process for the preparation of a compound of general formula II: ##STR1## wherein R.sup.1 is hydrogen, or C.sub.1 -C.sub.10 hydrocarbyl or heterocyclyl having 3 to 8 ring atoms, either of which may optionally be substituted; each R.sup.2, R.sup.3, R.sup.4 and R.sup.5 is independently hydrogen or C.sub.1 -C.sub.4 alkyl; A is an optionally substituted aromatic or heteroaromatic ring system; and R.sup.21 is hydrogen, halogen, OH or OCONHR.sup.1, wherein R.sup.1 is as defined above; the process comprising cyclizing a compound of general formula III: ##STR2## wherein A, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.21 are as defined in general formula II and R.sup.25 is a leaving group such as a halogen atom; under basic conditions.Type: GrantFiled: May 24, 1996Date of Patent: September 23, 1997Assignee: Zeneca LimitedInventors: John Michael Cox, Kevin James Gillen, Russell Martin Ellis, Shaheen Khatoon Vohra, Stephen Christopher Smith, Ian Richard Matthews
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Patent number: 5658858Abstract: The invention relates to 4-benzoylisoxazole compounds, compositions containing them, a process for preparation, and their use as herbicides.Type: GrantFiled: September 6, 1996Date of Patent: August 19, 1997Assignee: Rhone-Poulenc Argriculture LimitedInventors: Angela Jacqueline Bailey, Michael Gingell, David William Hawkins
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Patent number: 5656657Abstract: 3-amino-5-carbonylchromans, as well as enantiomers and salts thereof are disclosed. Pharmaceutical compositions containing the compounds as active ingredients are also disclosed. The compounds are useful in the treatment of 5-hydroxytryptamine-mediated disorders of the central nervous system.Type: GrantFiled: May 30, 1995Date of Patent: August 12, 1997Assignee: Astra AktiebolagInventors: Eva Maria Hammarberg, Lars George Johansson, Lars-Gunnar Larsson, Rolf Noreen, Lucy Anna Renyi, Svante Bertil Ross, Daniel Dungan Sohn, Bjorn Eric Svensson, Seth-Olov Thorberg
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Patent number: 5656573Abstract: The invention relates to 4-substituted isoxazole derivatives of formula I: ##STR1## wherein R, R.sup.1, R.sup.2, Q and n have the meanings defined in the description, which possess valuable herbicidal properties.Type: GrantFiled: June 2, 1995Date of Patent: August 12, 1997Assignee: Rhone-Poulenc Agriculture Ltd.Inventors: David Alan Roberts, Susan Mary Cramp, Paul Alfred Cain, Derek Ian Wallis, Jean-Paul Bulot, Gillian Mary Little, Brian Malcolm Luscombe
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Patent number: 5643933Abstract: This invention is in the field of antiinflammatory pharmaceutical agents and specifically relates to compounds, compositions and methods for treating disorders mediated by cyclooxygenase-2 or 5-lipoxygenase, such as inflammation.Type: GrantFiled: June 2, 1995Date of Patent: July 1, 1997Assignee: G. D. Searle & Co.Inventors: John J. Talley, James A. Sikorski, Bryan H. Norman, Roland S. Rogers, deceased, Balekudru Devadas, Matthew J. Graneto, Jeffery S. Carter
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Patent number: 5639772Abstract: 3-amino-5-aryl- and 5-heteroarylchromans, as well as enantiomers and salts thereof are disclosed. Pharmaceutical compositions containing the compounds as active ingredients are also disclosed. The compounds are useful in the treatment of 5-hydroxytryptamine-mediated disorders of the central nervous system.Type: GrantFiled: May 30, 1995Date of Patent: June 17, 1997Assignee: Astra AktiebolagInventors: Eva Maria Hammarberg, Lars George Johansson, Lars-Gunnar Larsson, Rolf Noreen, Lucy Anna Renyi, Svante Bertil Ross, Daniel Dungan Sohn, Bjorn Eric Svensson, Seth-Olov Thorberg
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Patent number: 5633272Abstract: A class of substituted isoxazolyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula II ##STR1## wherein R.sup.1 is selected from hydroxyl, lower alkyl, carboxyl, lower carboxyalkyl, lower aminocarbonylalkyl, lower alkoxycarbonylalkyl, lower aralkyl, lower alkoxyalkyl, lower aralkoxyalkyl, lower alkylthioalkyl, lower aralkylthioalkyl, lower alkylaminoalkyl, lower aryloxyalkyl, lower arylthioalkyl, lower haloalkyl, lower hydroxylalkyl, cycloalkyl, cycloalkylalkyl, and aralkyl; wherein R.sup.3 is selected from cycloalkyl, cycloalkenyl, aryl, and heteroaryl; wherein R.sup.Type: GrantFiled: June 7, 1995Date of Patent: May 27, 1997Inventors: John J. Talley, David L. Brown, Srinivasan Nagarajan, Jeffery S. Carter, Richard M. Weier, Michael A. Stealey, Paul W. Collins, Roland S. Rogers, deceased, Karen Seibert
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Patent number: 5622989Abstract: 6-Amino-benzofuryl- and thienyl-derivatives can be prepared by reacting appropriate amino-substituted benzoyl phenols with appropriate substituted acetophenones and subsequent modification of the substituents. The compounds are useful for the treatment of actual and chronic inflammatory diseases, particularly of the airways and the gastro-intestinal tract.Type: GrantFiled: May 23, 1995Date of Patent: April 22, 1997Assignee: Bayer AktiengesellschaftInventors: Gabriele Br aunlich, R udiger Fischer, Mazen Es-Sayed, Rudolf Hanko, Stephen Tudhope, Graham Sturton, Trevor Abram, Wendy J. McDonald-Gibson, Mary F. Fitzgerald
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Patent number: 5622983Abstract: Novel unnatural dipeptoids of .alpha.-substituted Trp-Phe derivatives useful as agents in the treatment of obesity, hypersecretion of gastric acid in the gut, gastrin-dependent tumors, colorectal tumors, or as antipsychotics are disclosed. Further the compounds are antianxiety agents, antiulcer agents, antidepressant agents, and are agents useful for preventing the withdrawal response produced by chronic treatment or use followed by chronic treatment followed by withdrawal from nicotine, diazepam, alcohol, cocaine, caffeine, or opiods. Also disclosed are pharmaceutical compositions and methods of treatment using the dipeptoids as well as processes for preparing them and novel intermediates useful in their preparation. An additional feature of the invention is the use of the subject compounds to prepare pharmaceutical and diagnostic compositions.Type: GrantFiled: May 22, 1995Date of Patent: April 22, 1997Assignee: Warner-Lambert CompanyInventors: David C. Horwell, Martyn C. Pritchard, Edward Roberts, Reginald S. Richardson, Julian Aranda
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Patent number: 5604256Abstract: Compounds of formula (I): ##STR1## (in which: R is hydrogen, methyl or hydroxy; X is alkyl, alkenyl, cycloalkyl, aryl, aralkyl, or a heterocyclic group; A is a single bond, or an alkylene, alkenylene, alkynylene or alkadienylene group; Y is hydrogen, aryl, cycloalkyl or a heterocyclic group) have the ability to inhibit the biosynthesis of cholesterol, and can thus be used for the treatment and prophylaxis of diseases relating to high blood cholesterol levels.Type: GrantFiled: December 14, 1994Date of Patent: February 18, 1997Assignee: Sankyo Company, LimitedInventors: Hiroshi Kogen, Masaaki Kurabayashi, Teiichiro Koga, Toru Komai, Haruo Iwabuchi
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Patent number: 5602160Abstract: Aminoketone derivative compounds containing a heterocyclic ring bonded to an aminoketone moiety and useful as effective ingredients of centrally acting muscle relaxants and pollakiurea curing agents.(+)3-phenyl-5-[2-(1-pyrrolidinylmethyl)butyryl] isoxazole, which has a more remarkable central muscle relaxant action as compared with its racemic modification, can be effectively separated from the racemic modification using optically active 10-camphorsulfonic acid as the agent for the optical resolution.Type: GrantFiled: April 17, 1995Date of Patent: February 11, 1997Assignee: Mitsui Toatsu Chemicals IncorporatedInventors: Hideki Tanada, Kazuya Sakai, Seitaro Kajiya, Norio Ohto, Kazutoshi Horikomi, Akira Matsubara, Hideshi Shimizu, Akira Mizuchi
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Patent number: 5580893Abstract: Nitroxyalkylamide compounds having the formula: R.sup.1 --(A).sub.n --CONH--B'--ONO.sub.2 wherein R.sup.1 is an optionally substituted furyl, furyloxy, thienyl, thienyloxy, isoxazolyl, phenoxy, phenylthio or 1,4-dibenzodioxanyl, A is a C.sub.1 -C.sub.4 alkylene group; B' is a C.sub.1 -C.sub.4 alkylene group; and n is 0 or 1. The compounds of the present invention have a desirable vasodilator action for collateral vessels and an anti-anginal action, and are useful as therapeutic agents for treating angina pectoris.Type: GrantFiled: July 25, 1994Date of Patent: December 3, 1996Assignee: Sankyo Company, LimitedInventors: Sadao Ishihara, Fujio Saito, Mitsuru Kataoka, Hiroyuki Koike, Shigeki Miyake, Hiroshi Mizuno
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Patent number: 5576270Abstract: The invention pertains to isoxazolecarboxamides of the formula I ##STR1## where R.sup.1 is alkyl, cycloalkyl, alkoxyalkyl, alkenyl, alkynyl, phenyl or unsubstituted or substituted benzyl,R.sup.2 is hydrogen or alkyl andR.sup.3 is alkyl, cycloalkyl, alkenyl, alkynyl, phenyl or unsubstituted or substituted benzyl,and the plant-tolerated salts of those compounds in which R.sup.2 is hydrogen, their preparation and their use.Type: GrantFiled: September 29, 1994Date of Patent: November 19, 1996Assignee: BASF AktiengesellschaftInventors: Volker Maywald, Thomas Kuekenhoehner, Peter Muenster, Wolfgang von Deyn, Helmut Walter, Matthias Gerber, Karl-Otto Westphalen, Uwe Kardorff
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Patent number: 5571923Abstract: Novel 1-alkyl-, 1-alkenyl-, and 1-alkynylaryl-2-amino-1,3-propanediols, intermediates and processes for the preparation thereof, and methods of reducing inflammation and cell proliferation, and relieving memory dysfunction, and inhibiting bacterial and fungal growth are disclosed.Type: GrantFiled: April 21, 1995Date of Patent: November 5, 1996Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: John J. Tegeler, Barbara S. Rauckman, Russell R. L. Harner, Brian S. Freed, Gregory H. Merriman
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Patent number: 5563158Abstract: This invention relates to novel compounds containing basic and acidic termini, pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of platelet aggregation, as thrombolytics, and/or for the treatment of thromboembolic disorders.Type: GrantFiled: November 22, 1994Date of Patent: October 8, 1996Assignee: The Dupont Merck Pharmaceutical CompanyInventors: William F. DeGrado, Chu-Biao Xue
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Patent number: 5550280Abstract: Compounds of the formula ##STR1## wherein X is O or S;Y is O or S;R.sup.1 is hydrogen, halogen, C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy;R.sup.2 is hydrogen, halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.2 -C.sub.4 alkenyl, C.sub.2 -C.sub.4 alkenyloxy, C.sub.2 -C.sub.4 alkynyl, C.sub.2 -C.sub.4 alkynyloxy, mono-, di- or tri-halomethyl, trifluoromethoxy, C.sub.1 -C.sub.4 alkylthio, C.sub.3 -C.sub.4 branched alkylthio, nitro, or cyano;R.sup.3 is hydrogen, halogen, methyl, mono-, di- or tri-halomethyl;R.sup.4 isa) C.sub.3 -C.sub.8 cycloalkyl substituted by one or more C.sub.1 -C.sub.4 alkyl, preferably one or two methyl;orb) ##STR2## wherein R.sup.6 and R.sup.7 are independently, hydrogen or linear or branched, C.sub.1 -C.sub.4 alkyl, C.sub.2 -C.sub.4 alkenyl, or C.sub.2 -C.sub.4 alkynyl, and R.sup.8 is C.sub.3 -C.sub.8 cycloalkyl substituted by one or more C.sub.1 -C.sub.4 alkyl; andR.sup.5 is an acyclic or cyclic side chain as defined herein.Type: GrantFiled: November 30, 1994Date of Patent: August 27, 1996Assignee: Uniroyal Chemical Ltd./ Uniroyal Chemical LteeInventors: Dong Dao-Cong, William A. Harrison
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Patent number: 5547984Abstract: Certain N-acetonyl-substituted-amides of the formula: ##STR1## wherein A is a heterocycle, a phenylalkyl, a phenylalkoxy, naphthyl, cycloalkyl, alkoxyalkyl, alkyl, haloalkyl or alkenyl group; X, Y and Z are selected from the group consisting of hydrogen, halo, cyano, thiocyano, isothiocyano, methylsulfonyloxy, thio(C.sub.1 -C.sub.2)alkyl, (C.sub.1 -C.sub.2)alkoxy, carbamoyl, dithiocarbamoyl, hydroxy, azide, trifluoromethylcarboxy, (C.sub.1 -C.sub.4)alkylcarbonyloxy, phenylcarbonyloxy, phenoxy, thiophenyl, imidazolyl or triazolyl group as described herein; R.sup.1 and R.sup.2 are each independently a hydrogen atom or a (C.sub.1 -C.sub.6)alkyl group; and compositions containing these amides are fungicidally active, particularly against phytopathogenic fungi.Type: GrantFiled: June 6, 1995Date of Patent: August 20, 1996Assignee: Rohm and Haas CompanyInventor: Ashok K. Sharma
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Patent number: 5543416Abstract: Cyanoisoxazoles of the formula Ia or Ib ##STR1## where R.sup.1 is hydrogen, alkyl, cycloalkyl, phenyl; R.sup.2 is hydrogen, alkyl, cycloalkyl and R.sup.3 is alkoxy, alkyl, cycloalkyl, cycloalkenyl, alkenyl, alkynyl or phenyl, it being possible for the organic radicals mentioned under R.sup.1, R.sup.2 and R.sup.3 to be substituted in each case. The compounds of the Formula Ia or Ib are useful as herbicides.Type: GrantFiled: February 22, 1995Date of Patent: August 6, 1996Assignee: BASF AktiengesellschaftInventors: Peter M unster, Klaus Ditrich, Gerhard Hamprecht, Matthias Gerber, Karl-Otto Westphalen, Helmut Walter, Rudolf Karl