Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To Ring Carbon Of The Oxazole Ring By Nonionic Bonding Patents (Class 548/248)
  • Patent number: 6083986
    Abstract: Compounds useful as potassium channel inhibitors and especially useful for the treatment of cardiac arrhythmias and cell proliferative disorders are described.
    Type: Grant
    Filed: July 15, 1997
    Date of Patent: July 4, 2000
    Assignees: ICAgen, Inc., Eli Lilly & Company
    Inventors: 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
  • Patent number: 6075026
    Abstract: 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: Grant
    Filed: April 21, 1997
    Date of Patent: June 13, 2000
    Assignee: Molecular Geriatrics, Corp.
    Inventors: John Francis DeBernardis, Daniel Joseph Kerkman, Raymond Paul Zinkowski
  • Patent number: 6069115
    Abstract: 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: Grant
    Filed: November 12, 1997
    Date of Patent: May 30, 2000
    Assignee: Rhone-Poulenc Agrochimie
    Inventors: Ken Pallett, Richard Derose, Bernard Pelissier, Alain Sailland, Thomas Edward Vrabel
  • Patent number: 6060494
    Abstract: 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: Grant
    Filed: August 6, 1998
    Date of Patent: May 9, 2000
    Assignee: Hoechst Marion Roussel Deutschland GmbH
    Inventors: Holger Faasch, Udo Hedtmann, Uwe Westenfelder, Erich Paulus
  • Patent number: 6037312
    Abstract: 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: Grant
    Filed: February 3, 1999
    Date of Patent: March 14, 2000
    Assignee: Idemitsu Kosan Co., Ltd.
    Inventors: Yoriyuki Takashima, Hideki Kamano, Masashi Sakamoto
  • Patent number: 6022868
    Abstract: 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: Grant
    Filed: December 19, 1997
    Date of Patent: February 8, 2000
    Assignee: Novo Nordisk Als
    Inventors: Preben Houlberg Olesen, John Bondo Hansen
  • Patent number: 6020371
    Abstract: 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: Grant
    Filed: December 16, 1997
    Date of Patent: February 1, 2000
    Assignee: Agouron Pharmaceuticals, Inc.
    Inventors: Peter S. Dragovich, Thomas J. Prins, Ru Zhou
  • Patent number: 6013805
    Abstract: The invention relates to intermediates to herbicidal compounds of formulae (Ia), (Ib) or (Ic): ##STR1##
    Type: Grant
    Filed: September 29, 1998
    Date of Patent: January 11, 2000
    Assignee: Rhone-Poulenc Agriculture Ltd
    Inventor: David William Hawkins
  • Patent number: 5998613
    Abstract: 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: Grant
    Filed: August 5, 1997
    Date of Patent: December 7, 1999
    Assignee: H. Lundbeck A/S
    Inventors: Erik Falch, Jens Kristian Perregaard, Arne Schousboe, Povl Krogsgaard-Larsen, Bente Frolund, Sibylle Moltzen Lenz
  • Patent number: 5985799
    Abstract: 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: Grant
    Filed: May 12, 1998
    Date of Patent: November 16, 1999
    Assignee: E.I. du Pont de Nemours and Company
    Inventor: Chi-Ping Tseng
  • Patent number: 5977149
    Abstract: 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: Grant
    Filed: January 14, 1998
    Date of Patent: November 2, 1999
    Assignee: E. I. du Pont de Nemours and Company
    Inventors: Richard James Brown, King-Mo Sun, Deborah Ann Frasier
  • Patent number: 5977151
    Abstract: 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: Grant
    Filed: January 23, 1998
    Date of Patent: November 2, 1999
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Stefan Mullner, Bernd Kirschbaum, Wilfried Schwab
  • Patent number: 5965740
    Abstract: 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: Grant
    Filed: February 20, 1998
    Date of Patent: October 12, 1999
    Assignee: Shionogi & Co., Ltd.
    Inventors: Hiroyuki Kai, Akira Takase, Toshikazu Ohtsuka
  • Patent number: 5962487
    Abstract: 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: Grant
    Filed: December 16, 1997
    Date of Patent: October 5, 1999
    Assignee: Agouron Pharmaceuticals, Inc.
    Inventors: Stephen E. Webber, Peter S. Dragovich, Thomas J. Prins, Ethel S. Littlefield, Joseph T. Marakovits, Robert E. Babine
  • Patent number: 5935973
    Abstract: 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: Grant
    Filed: January 5, 1998
    Date of Patent: August 10, 1999
    Assignee: Knoll Aktiengesellschaft
    Inventors: Alan Martin Birch, David John Heal, Frank Kerrigan, Keith Frank Martin, Patricia Lesley Needham, Bruce Jeremy Sargent
  • Patent number: 5885983
    Abstract: 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: Grant
    Filed: April 23, 1997
    Date of Patent: March 23, 1999
    Assignee: Bristol-Myers Squibb Company
    Inventors: Scott A. Biller, John K. Dickson, Jr.
  • Patent number: 5859257
    Abstract: 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: Grant
    Filed: August 14, 1996
    Date of Patent: January 12, 1999
    Assignee: G. D. Searle & Co.
    Inventor: John J Talley
  • Patent number: 5856274
    Abstract: 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: Grant
    Filed: September 14, 1995
    Date of Patent: January 5, 1999
    Assignee: Rhone-Poulenc Agriculture Limited
    Inventors: Susan Mary Cramp, Claude Lambert, Derek Ian Wallis, Thomas Yarwood
  • Patent number: 5849928
    Abstract: The invention relates to compounds of formulae (Ia), (Ib) or (Ic): ##STR1## and to their use as herbicides.
    Type: Grant
    Filed: March 21, 1997
    Date of Patent: December 15, 1998
    Assignee: Rhone-Poulenc Agriculture Limited
    Inventor: David William Hawkins
  • Patent number: 5849736
    Abstract: 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: Grant
    Filed: May 31, 1995
    Date of Patent: December 15, 1998
    Assignee: The DuPont Merck Pharmaceutical Company
    Inventors: 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
  • Patent number: 5834468
    Abstract: 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: Grant
    Filed: July 2, 1996
    Date of Patent: November 10, 1998
    Assignee: Zeneca Limited
    Inventors: Gloria Anne Breault, John Oldfield, Howard Tucker, Peter Warner
  • Patent number: 5814627
    Abstract: 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: Grant
    Filed: November 19, 1996
    Date of Patent: September 29, 1998
    Assignee: Hoechst Aktienegesellschaft
    Inventors: Wilfried Schwab, Hiristo Anagnostopulos, Robert Ryder Bartlett, Rudolf Schleyerbach, Klaus Ulrich Weithmann
  • Patent number: 5780393
    Abstract: 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: Grant
    Filed: August 23, 1996
    Date of Patent: July 14, 1998
    Assignee: American Cyanamid Company
    Inventor: Trevor W. Newton
  • Patent number: 5760066
    Abstract: 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: Grant
    Filed: April 19, 1996
    Date of Patent: June 2, 1998
    Assignee: Sugen, Inc.
    Inventor: Peng Cho Tang
  • Patent number: 5760244
    Abstract: 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: Grant
    Filed: July 28, 1997
    Date of Patent: June 2, 1998
    Assignee: Shionogi & Co., Ltd.
    Inventors: Susumu Takada, Nobuo Chomei, Masaaki Uenaka
  • Patent number: 5750543
    Abstract: 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: Grant
    Filed: February 1, 1996
    Date of Patent: May 12, 1998
    Assignee: The Procter & Gamble Company
    Inventors: Laurence Ichih Wu, John Michael Janusz
  • Patent number: 5747424
    Abstract: 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: Grant
    Filed: May 1, 1997
    Date of Patent: May 5, 1998
    Assignee: Rhone-Poulenc Agriculture Ltd.
    Inventors: David Alan Roberts, Susan Mary Cramp, Derek Ian Wallis, Jean-Paul Bulot
  • Patent number: 5741801
    Abstract: 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: Grant
    Filed: November 22, 1995
    Date of Patent: April 21, 1998
    Assignee: SmithKline Beecham plc
    Inventors: Francis David King, Laramie Mary Gaster, Keith Raymond Mulholland
  • Patent number: 5703017
    Abstract: 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: Grant
    Filed: October 19, 1995
    Date of Patent: December 30, 1997
    Assignee: BASF Aktiengesellschaft
    Inventors: Ernst Baumann, Joachim Rheinheimer, Uwe Josef Vogelbacher, Matthias Bratz, Hans Theobald, Matthias Gerber, Karl-Otto Westphalen, Helmut Walter, Wilhelm Rademacher
  • Patent number: 5696271
    Abstract: 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: Grant
    Filed: August 7, 1996
    Date of Patent: December 9, 1997
    Assignee: Shionogi & Co., Ltd.
    Inventors: Susumu Takada, Nobuo Chomei, Masaaki Uenaka
  • Patent number: 5693804
    Abstract: 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: Grant
    Filed: November 17, 1994
    Date of Patent: December 2, 1997
    Assignee: Molecular Geriatrics Corporation
    Inventors: John Francis DeBernardis, Daniel Joseph Kerkman, Raymond Paul Zinkowski
  • Patent number: 5691366
    Abstract: 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: Grant
    Filed: October 31, 1995
    Date of Patent: November 25, 1997
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Masayuki Kato, Shigetaka Nishino, Mitsuko Hamano, Hisashi Takasugi
  • Patent number: 5670656
    Abstract: 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: Grant
    Filed: May 24, 1996
    Date of Patent: September 23, 1997
    Assignee: Zeneca Limited
    Inventors: John Michael Cox, Kevin James Gillen, Russell Martin Ellis, Shaheen Khatoon Vohra, Stephen Christopher Smith, Ian Richard Matthews
  • Patent number: 5658858
    Abstract: The invention relates to 4-benzoylisoxazole compounds, compositions containing them, a process for preparation, and their use as herbicides.
    Type: Grant
    Filed: September 6, 1996
    Date of Patent: August 19, 1997
    Assignee: Rhone-Poulenc Argriculture Limited
    Inventors: Angela Jacqueline Bailey, Michael Gingell, David William Hawkins
  • Patent number: 5656657
    Abstract: 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: Grant
    Filed: May 30, 1995
    Date of Patent: August 12, 1997
    Assignee: Astra Aktiebolag
    Inventors: 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
  • Patent number: 5656573
    Abstract: 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: Grant
    Filed: June 2, 1995
    Date of Patent: August 12, 1997
    Assignee: 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
  • Patent number: 5643933
    Abstract: 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: Grant
    Filed: June 2, 1995
    Date of Patent: July 1, 1997
    Assignee: 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
  • Patent number: 5639772
    Abstract: 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: Grant
    Filed: May 30, 1995
    Date of Patent: June 17, 1997
    Assignee: Astra Aktiebolag
    Inventors: 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
  • Patent number: 5633272
    Abstract: 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: Grant
    Filed: June 7, 1995
    Date of Patent: May 27, 1997
    Inventors: 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
  • Patent number: 5622989
    Abstract: 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: Grant
    Filed: May 23, 1995
    Date of Patent: April 22, 1997
    Assignee: Bayer Aktiengesellschaft
    Inventors: Gabriele Br aunlich, R udiger Fischer, Mazen Es-Sayed, Rudolf Hanko, Stephen Tudhope, Graham Sturton, Trevor Abram, Wendy J. McDonald-Gibson, Mary F. Fitzgerald
  • Patent number: 5622983
    Abstract: 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: Grant
    Filed: May 22, 1995
    Date of Patent: April 22, 1997
    Assignee: Warner-Lambert Company
    Inventors: David C. Horwell, Martyn C. Pritchard, Edward Roberts, Reginald S. Richardson, Julian Aranda
  • Patent number: 5604256
    Abstract: 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: Grant
    Filed: December 14, 1994
    Date of Patent: February 18, 1997
    Assignee: Sankyo Company, Limited
    Inventors: Hiroshi Kogen, Masaaki Kurabayashi, Teiichiro Koga, Toru Komai, Haruo Iwabuchi
  • Patent number: 5602160
    Abstract: 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: Grant
    Filed: April 17, 1995
    Date of Patent: February 11, 1997
    Assignee: Mitsui Toatsu Chemicals Incorporated
    Inventors: Hideki Tanada, Kazuya Sakai, Seitaro Kajiya, Norio Ohto, Kazutoshi Horikomi, Akira Matsubara, Hideshi Shimizu, Akira Mizuchi
  • Patent number: 5580893
    Abstract: 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: Grant
    Filed: July 25, 1994
    Date of Patent: December 3, 1996
    Assignee: Sankyo Company, Limited
    Inventors: Sadao Ishihara, Fujio Saito, Mitsuru Kataoka, Hiroyuki Koike, Shigeki Miyake, Hiroshi Mizuno
  • Patent number: 5576270
    Abstract: 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: Grant
    Filed: September 29, 1994
    Date of Patent: November 19, 1996
    Assignee: BASF Aktiengesellschaft
    Inventors: Volker Maywald, Thomas Kuekenhoehner, Peter Muenster, Wolfgang von Deyn, Helmut Walter, Matthias Gerber, Karl-Otto Westphalen, Uwe Kardorff
  • Patent number: 5571923
    Abstract: 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: Grant
    Filed: April 21, 1995
    Date of Patent: November 5, 1996
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: John J. Tegeler, Barbara S. Rauckman, Russell R. L. Harner, Brian S. Freed, Gregory H. Merriman
  • Patent number: 5563158
    Abstract: 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: Grant
    Filed: November 22, 1994
    Date of Patent: October 8, 1996
    Assignee: The Dupont Merck Pharmaceutical Company
    Inventors: William F. DeGrado, Chu-Biao Xue
  • Patent number: 5550280
    Abstract: 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: Grant
    Filed: November 30, 1994
    Date of Patent: August 27, 1996
    Assignee: Uniroyal Chemical Ltd./ Uniroyal Chemical Ltee
    Inventors: Dong Dao-Cong, William A. Harrison
  • Patent number: 5547984
    Abstract: 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: Grant
    Filed: June 6, 1995
    Date of Patent: August 20, 1996
    Assignee: Rohm and Haas Company
    Inventor: Ashok K. Sharma
  • Patent number: 5543416
    Abstract: 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: Grant
    Filed: February 22, 1995
    Date of Patent: August 6, 1996
    Assignee: BASF Aktiengesellschaft
    Inventors: Peter M unster, Klaus Ditrich, Gerhard Hamprecht, Matthias Gerber, Karl-Otto Westphalen, Helmut Walter, Rudolf Karl