Chalcogen Bonded Directly To Ring Carbon Of The Oxazole Ring Patents (Class 548/243)
  • Patent number: 6048885
    Abstract: A compound represented by general formula (I) or a salt thereof, a process for producing the same, an intermediate for the production thereof, and a bactericide (fungicide) containing the same as the active ingredient wherein R.sup.1 represent optionally substituted aryl, optionally substituted heterocycle, mono- or di-substituted methyleneamino, optionally substituted (substituted imino)methyl, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, substituted carbonyl or substituted sulfonyl; R.sup.2 represents alkyl, alkenyl, alkynyl or cycloalkyl; R.sup.3 represents optionally substituted heterocycle; R.sup.4 represents hydrogen, alkyl, alkoxy, halogen, nitro, cyano or haloalkyl; M represents oxygen, S(O)i (i being 0, 1 or 2), NR.sup.16 (R.sup.16 being hydrogen, alkyl or acyl) or a single bond; n represents 0 or 1, provided n represent 1 when R3 represents imidazol-1-yl or 1H-1, 2, 4-triazol-1-yl; and the symbol .about.
    Type: Grant
    Filed: August 21, 1996
    Date of Patent: April 11, 2000
    Assignee: Shionogi & Co., Ltd.
    Inventors: Akira Takase, Hiroyuki Kai, Kuniyoshi Nishida, Tsuneo Iwakawa, Kazuo Ueda, Michio Masuko
  • Patent number: 6043377
    Abstract: The present invention concerns novel imidazol derivatives of the formula (I), ##STR1## in which R.sup.1, R.sup.2, R.sup.3 and A have the meanings given in the description,and the acid addition salts and metal salt complexes, several processes for the production of the novel substances and their use for combating undesirable micro-organisms in plant and material protection.
    Type: Grant
    Filed: December 8, 1998
    Date of Patent: March 28, 2000
    Assignee: Bayer Aktiengesellschaft
    Inventors: Lutz Assmann, Hans-Ludwig Elbe, Ralf Tiemann, Markus Heil, Klaus Stenzel
  • Patent number: 6030970
    Abstract: Novel to isooxazoles, oxazoles, thiazoles, isothiazoles and imidazoles, pharmaceutical compositions containing these compounds and their use as endothelin receptor antagonists are described.
    Type: Grant
    Filed: February 2, 1998
    Date of Patent: February 29, 2000
    Assignee: Smithkline Beecham Corporation
    Inventors: John Duncan Elliott, Juan Ignacio Luengo, Jia-Ning Xiang
  • Patent number: 6025382
    Abstract: This application relates to the use as thrombin inhibitors, coagulation inhibitors and thromboembolic disorder agents of diamines of formula I as defined herein. It also provides novel compounds of formula I, processes and intermediates for their preparation, and pharmaceutical formulations comprising the novel compounds of formula I.
    Type: Grant
    Filed: April 30, 1997
    Date of Patent: February 15, 2000
    Assignee: Eli Lilly and Company
    Inventors: Jolie Anne Bastian, Nickolay Yuri Chirgadze, Michael Lyle Denney, Matthew Joseph Fisher, Robert James Foglesong, Richard Waltz Harper, Mary George Johnson, Valentine Joseph Klimkowski, Todd Jonathan Kohn, Ho-Shen Lin, Michael Patrick Lynch, Jefferson Ray McCowan, Alan David Palkowitz, Michael Enrico Richett, Daniel Jon Sall, Gerald Floyd Smith, Kumiko Takeuchi, Jennifer Marie Tinsley, Minsheng Zhang
  • Patent number: 6022977
    Abstract: The present invention relates generally to a novel method for preparation of substituted isoxazolin-5-yl acetic acid in high optical purity from a stereoisomeric mixture of an esterified substituted isoxazolin-5-yl acetate. The products are useful in the synthesis of compounds for pharmaceuticals, especially the treatment of thrombolytic disorders, and agricultural products.
    Type: Grant
    Filed: March 25, 1998
    Date of Patent: February 8, 2000
    Assignee: DuPont Pharmaceuticals Company
    Inventors: Lin-Hua Zhang, Luigi Anzalone, Jaan A. Pesti, Jianguo Yin
  • Patent number: 6020354
    Abstract: New halogenobenzimidazoles of the formula in whichA, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and X have the meanings given in the description,and their acid addition salts and metal salt complexes,a process for their preparation and their use as microbicides in crop protection and in the protection of materials.New intermediates of the formula ##STR1## in which R.sup.12 -R.sup.17 and X have the meanings given in the description,and processes for the preparation of these substances.
    Type: Grant
    Filed: January 28, 1998
    Date of Patent: February 1, 2000
    Assignee: Bayer Aktiengesellschaft
    Inventors: Lutz Assmann, Albrecht Marhold, Ralf Tiemann, Klaus Stenzel
  • Patent number: 6015909
    Abstract: An arylidene compound is represented by the following formula (I): ##STR1## in which L.sup.1 is a divalent linking group comprising at least one --NH-- and at least one of --CO-- and --SO.sub.2 --; L.sup.2 is monomethine, trimethine or pentamethine; R.sup.1 is an alkyl group, an aryl group or a heterocyclic group; each of R.sup.2 and R.sup.3 independently is hydrogen, an alkyl group or an aryl group, and the number of the total carbon atoms contained in R.sup.2 and R.sup.3 is not more than 20. A silver halide photographic material containing an arylidene dye is also disclosed.
    Type: Grant
    Filed: September 3, 1997
    Date of Patent: January 18, 2000
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Toshiki Fujiwara, Seiji Yamashita, Keiichi Suzuki
  • 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: 6004955
    Type: Grant
    Filed: August 12, 1998
    Date of Patent: December 21, 1999
    Assignee: DuPont Pharmaceuticals Company
    Inventors: Fuqiang Jin, Pasquale Nicholas Confalone
  • Patent number: 6005116
    Abstract: Isoxazole compounds having the following general formula: ##STR1## wherein R.sup.1 represents an optionally substituted aryl group or aromatic heterocyclic group; R.sup.2 represents a hydrogen atom, a halogen atom, an optionally substituted alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, a cycloalkenyl group, an alkoxy group, a cyano group, a carboxyl group, an alkanoyl group, an alkoxycarbonyl group or an optionally substituted carbamoyl group; R.sup.3 represents an optionally substituted amino group or a saturated heterocyclic group; X represents an oxygen atom or a sulfur atom; and n is an integer of from 2 to 6. These compounds have excellent monoamine oxidase inhibitory activity and are useful as a therapeutic agent or a preventive agent against nervous diseases such as depression.
    Type: Grant
    Filed: August 26, 1998
    Date of Patent: December 21, 1999
    Assignee: Sankyo Company, Limited
    Inventors: Koichi Kojima, Junichi Sakai, Naozumi Samata, Masao Kozuka, Kenji Yoshimi, Tsugio Kaneko
  • 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: 5985903
    Abstract: Novel benzotriazoles of the formula ##STR1## in which R, X.sup.1, X.sup.2, X.sup.3, X.sup.4 and Y have the meanings given in the description,and their acid addition salts and metal salt complexes,a process for the preparation of these substances and their use as microbicides in crop protection and in material protection.
    Type: Grant
    Filed: December 19, 1997
    Date of Patent: November 16, 1999
    Assignee: Bayer Aktiengesellschaft
    Inventors: Lutz Assmann, Ralf Tiemann, Martin Kugler, Heinrich Schrage, Klaus Stenzel
  • Patent number: 5962490
    Abstract: Thienyl-, furyl- and pyrrolyl-sulfonamides and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, N-(isoxazolyl)thienylsulfonamides, N-(isoxazolyl)-furylsulfonamides and N-(isoxazolyl)pyrrolylsulfonamides and methods using these sulfonamides for inhibiting the binding of an endothelin peptide to an endothelin receptor by contacting the receptor with the sulfonamide are provided. Methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these sulfonamides or prodrugs thereof that inhibit or increase the activity of endothelin are also provided.
    Type: Grant
    Filed: September 27, 1996
    Date of Patent: October 5, 1999
    Assignee: Texas Biotechnology Corporation
    Inventors: Ming Fai Chan, Chengde Wu, Bore Gowda Raju, Timothy Kogan, Adam Kois, Erik Joel Verner, Rosario Silvestre Castillo, Venkatachalapathi Yalamorri, Vitukudi Narayanaiyengar Balaji
  • Patent number: 5959119
    Abstract: By a novel process, 3,5-dimethylisoxazole-4-sulphonyl chloride is prepared by reacting 3,5-dimethylisoxazole initially with chlorosulphonic acid and then additionally with thionyl chloride at a temperature between 60.degree. C. and 110.degree. C.
    Type: Grant
    Filed: October 20, 1998
    Date of Patent: September 28, 1999
    Assignee: Bayer Aktiengesellschaft
    Inventors: Bernd Gallenkamp, Lothar Rohe
  • Patent number: 5952354
    Abstract: Inhibition of the enzymes cholesterol ester hydrolase (CEH) and/or acyl coenzyme A: cholesterol acyltransferase (ACAT) results in the inhibition of the esterification of cholesterol and are therefore implicated in the inhibition of absorption of cholesterol and thus can lower serum cholesterol levels. Compounds of the formula: ##STR1## where Z is ##STR2## or --Ar.sup.1 --(CR.dbd.CR).sub.1-3 --Ar.sup.2, --AR.sup.1 --NR.sup.7 --AR.sup.2 and A is a linking group inhibit the enzymes CEH and/or ACAT (in vitro) and inhibit absorption of cholesterol.
    Type: Grant
    Filed: July 21, 1993
    Date of Patent: September 14, 1999
    Assignee: American Home Products Corporation
    Inventors: Thomas Joseph Commons, Donald Peter Strike, Christa Marie LaClair
  • Patent number: 5939418
    Abstract: Isoxazolines, isothiazolines and pyrazolines which are inhibitors of Factor Xa, pharmaceutical compositions containing these compounds, and methods of using these compounds as anticoagulant agents for treatment and prevention of thromboembolic disorders. The compounds can be represented by the formula: ##STR1## where X is O, S or NR.sup.15.
    Type: Grant
    Filed: December 17, 1996
    Date of Patent: August 17, 1999
    Assignee: The DuPont Merck Pharmaceutical Company
    Inventors: Mimi Lifen Quan, John Wityak, Robert Anthony Galemmo, Jr., Petrus F. W. Stouten, James Russell Pruitt, Donald J. P. Pinto
  • 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: 5932583
    Abstract: Bis-oxime derivatives of the formula I ##STR1## W is oxygen or sulfur, and the other substituents defined as follows: R.sub.1 =hydrogen, C.sub.1 -C.sub.4 alkyl; cyclopropyl;R.sub.2 =hydrogen, C.sub.1 -C.sub.6 alkyl; halo(C.sub.1 -C.sub.6) alkyl; C.sub.2 -C.sub.6 alkoxyalkyl; C.sub.3 -C.sub.6 cycloalkyl; substituted or unsubstituted aryl; substituted or unsubstituted heteroaryl; cyano; C.sub.1 -C.sub.6 alkoxycarbonyl; C.sub.1 -C.sub.6 alkyl-S(O).sub.n ; substituted or unsubstituted aryl-S(O).sub.n ; C.sub.1 -C.sub.6 alkoxy; substituted or unsubstituted aryloxy; substituted or unsubstituted heteroaryloxy; unsubstituted or mono- to trimethyl-substituted heterocyclyl; substituted or unsubstituted aryl-C.sub.1 -C.sub.6 alkyl; substituted or unsubstituted heteroaryl-C.sub.1 -C.sub.6 alkyl;R.sub.3 =hydrogen; C.sub.1 -C.sub.6 alkyl; C.sub.1 -C.sub.6 haloalkyl having 1 to 5 halogen atoms; C.sub.1 -C.sub.4 alkoxy-C.sub.1 -C.sub.2 -alkyl; unsubstituted or mono- to trihalo-substituted C.sub.1 -C.sub.6 alkenyl; C.sub.
    Type: Grant
    Filed: December 23, 1997
    Date of Patent: August 3, 1999
    Assignee: Novartis Crop Protection, Inc.
    Inventors: Hugo Ziegler, Stephan Trah, Rene Zurfluh, Anthony Cornelius O'Sullivan
  • Patent number: 5932731
    Abstract: The present invention provides a process for preparing an aromatic or heteroaromatic thiol represented by the formula (2), the process comprising hydrolyzing an aromatic or heteroaromatic halogenated methyl sulfide represented by the formula (1)Ar.paren open-st.SCH.sub.3-m X.sub.m).sub.n (1)Ar.paren open-st.SH).sub.n (2)wherein Ar is an aromatic or heteroaromatic ring which has no substituent or which has an optional substituent or substituents, X is a halogen atom, m is an integer of 1 to 3 and n is 1 or 2.
    Type: Grant
    Filed: December 22, 1997
    Date of Patent: August 3, 1999
    Assignee: Sumitomo Seika Chemicals Co., Ltd.
    Inventors: Hiroshi Goda, Mikio Yamamoto, Jun-ichi Sakamoto, Hitoshi Karino
  • Patent number: 5929279
    Abstract: A process for the preparation of largely isomerically pure .alpha.-bisoximes of the formula IaR.sup.1 O--N.dbd.CR.sup.2 --CR.sup.3 .dbd.N--OR.sup.4 Iawhere the groups R.sup.1 O-- and R.sup.2 on the N.dbd.C bond are cis to one another and where the radicals have the following meanings:R.sup.1 and R.sup.4 are hydrogen or a C-organic radical;R.sup.2 is hydrogen, cyano, nitro, hydroxyl, amino, halogen or an organic radical which can be bonded to the structure directly or via an oxygen, sulfur or nitrogen atom;R.sup.3 is hydrogen, cyano, nitro, hydroxyl, amino, halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio, alkylamino, dialkylamino or cycloalkyl,from a mixture of the isomers of the a-bisoximes Ia and Ib ##STR1## is described.
    Type: Grant
    Filed: October 7, 1997
    Date of Patent: July 27, 1999
    Assignee: BASF Aktiengesellschaft
    Inventors: Ruth Muller, Remy Benoit, Herbert Bayer, Norbert Gotz, Hubert Sauter
  • Patent number: 5925663
    Abstract: Novel benzimidazole derivatives of the formula ##STR1## R.sup.1, R.sup.2, X.sup.1, X.sup.2, X.sup.3, X.sup.4 and Y are each as defined in the description,and metal salt complexes thereof,a process for preparing these compounds and their use as microbicides in crop protection and in teh protection of materials.
    Type: Grant
    Filed: October 3, 1997
    Date of Patent: July 20, 1999
    Assignee: Bayer Aktiengesellschaft
    Inventors: Lutz Assmann, Albrecht Marhold, Klaus Stenzel, Martin Kugler
  • Patent number: 5919944
    Abstract: Diketopyrrolopyrroles of formula I ##STR1## wherein R.sub.1 is a radical of formula II--Y--X--Z--Q (II),whereinY is --CR.sub.3 R.sub.4, --SO.sub.2 --, --CO--, --Si(Hal).sub.2 --, --POHal--, wherein R.sub.3 and R.sub.4 are each independently of the other hydrogen or C.sub.1 -C.sub.4 alkyl, and Hal is halogen,X is an unsubstituted or substituted carbocylic or heterocyclic arylene group, Z is a single bond, uninterrupted linear or branched C.sub.1 -C.sub.30 alkylene, or linear or branched C.sub.2 -C.sub.30 alkylene which is interrupted once or more than once by a hetero atom, --CH.dbd.CH--, --C.tbd.C--, --N.dbd.CH--, --CH.dbd.N-- or --NH--, or is C.sub.5 -C.sub.12 cycloalkylene,Q is a polyreactive functional group, andR.sub.2 is C.sub.1 -C.sub.6 alkyl, ##STR2## or R.sub.1, and R.sub.7 is hydrogen or C.sub.1 -C.sub.
    Type: Grant
    Filed: July 20, 1998
    Date of Patent: July 6, 1999
    Assignee: Ciba Specialty Chemicals Corporation
    Inventor: Sameer Eldin
  • Patent number: 5863865
    Abstract: This invention relates to 4-benzoylisoxazoles of formula (I) ##STR1## as well as herbicide compositions containing them and their use as herbicides.
    Type: Grant
    Filed: October 28, 1997
    Date of Patent: January 26, 1999
    Assignee: Zeneca Limited
    Inventors: David L. Lee, Nigel Barnes
  • 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: 5852007
    Abstract: The present invention is directed to (D)-amino acid containing inhibitors of cysteine or serine proteases. Methods for the use of the protease inhibitors are also described.
    Type: Grant
    Filed: February 6, 1997
    Date of Patent: December 22, 1998
    Assignee: Cephalon, Inc.
    Inventor: Sankar Chatterjee
  • Patent number: 5834508
    Abstract: A novel ketone derivative (I) which possesses a potent inhibitory activity against thiol protease such as papain, cathepsin B, cathepsin H, cathepsin L, calpain or the like with excellent properties regarding oral absorbance, tissue transference and cell membrane permeability, and are clinically useful in the treatment of various diseases such as muscular dystrophy, amyotrophy. Also provided are a process for producing the compound (I) and a pharmaceutical composition containing the same.
    Type: Grant
    Filed: February 6, 1997
    Date of Patent: November 10, 1998
    Assignee: Mitsubishi Chemical Corporation
    Inventors: Ryoichi Ando, Naoko Ando, Hirokazu Masuda, Yasuhiro Morinaka, Chizuko Takahashi, Yoshikuni Tamao, Akihiro Tobe
  • 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: 5824677
    Abstract: Disclosed are compounds having a straight or branched aliphatic hydrocarbon structure of formula I: ##STR1## In formula I, n is an integer from one to four and m is an integer from four to twenty. Independently, R.sub.1 and R.sub.2 are hydrogen, a straight or branched chain alkyl, alkenyl or alkynyl of up to twenty carbon atoms in length or --(CH.sub.2).sub.w R.sub.5. If R.sub.1 or R.sub.2 is --(CH.sub.2).sub.w R.sub.5, w may be an integer from one to twenty and R.sub.5 may be an hydroxyl, halo, C.sub.1-8 alkoxyl group or a substituted or unsubstituted carbocycle or heterocycle. Alternatively, R.sub.1 and R.sub.2 may jointly form a substituted or unsubstituted, saturated or unsaturated heterocycle having from four to eight carbon atoms, N being a hetero atom of the resulting heterocyle. R.sub.3 may be either hydrogen or C.sub.13. In the compounds, a total sum of carbon atoms comprising R.sub.1 or R.sub.2, (CH.sub.2).sub.n and (CH.sub.2).sub.m does not exceed forty. R.sub.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: October 20, 1998
    Assignee: Cell Therapeutics, Inc.
    Inventors: J. Peter Klein, Gail E. Underiner, Anil M. Kumar
  • Patent number: 5811441
    Abstract: This invention relates to improved isoxazoline compounds including, but not limited to N.sup.2 -(3,5-dimethylisoxazole-4-sulfonyl)-N.sup.3 -?3-(4-amidinophenyl)isoxazolin-5(R)-ylacetyl!-(S)-2,3-diaminopropionic acid, which are useful as antagonists of the platelet glycoprotein IIb/IIIa fibrinogen receptor complex, to pharmaceutical compositions containing 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: September 3, 1997
    Date of Patent: September 22, 1998
    Assignee: The DuPont Merck Pharmaceutical Company
    Inventors: Richard Eric Olson, John Wityak
  • Patent number: 5760059
    Abstract: This invention relates to compounds of formula ##STR1## or a salt, or metabolically labile ester thereof wherein R represents a group selected from halogen, alkyl, alkoxy, amino, alkylamino, dialkylamino, hydroxy, trifluoromethyl, trifluoromethoxy, nitro, cyano, SO.sub.2 R.sub.2 or COR.sub.2 wherein R.sub.2 represents hydroxy, methoxy, amino, alkylamino, or dialkylamino; m is zero or an integer 1 or 2;R.sub.1 represents a cycloalkyl, bridged cycloalkyl, heteroaryl, bridged heterocyclic or optionally substituted phenyl or fused bicyclic carbocylic group;A represents a C.sub.1-4 alkylene chain or the chain (CH.sub.2).sub.p Y(CH.sub.2).sub.q wherein Y is O, S(O)n or NR.sub.3 and which chains may be substituted by one or two groups selected from C.sub.1-6 alkyl optionally substituted by hydroxy, amino, alkylamino or dialkylamino, or which chains may be substituted by the group .dbd.O;R.sub.
    Type: Grant
    Filed: March 29, 1996
    Date of Patent: June 2, 1998
    Assignee: Glaxo Wellcome SpA
    Inventors: Alfredo Cugola, Romano DiFabio, Giorgio Pentassuglia
  • 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: 5747513
    Abstract: Compounds of the formula: ##STR1## wherein R is a hydrogen atom or an OY group; R.sub.1 is a hydrogen atom or in OY' group; R.sub.2 is a hydrogen atom or an OY" group; provided that at lent one among R, R.sub.1 and R.sub.2 is hydrogen but R, R.sub.1, and R.sub.2 are not contemporaneously hydrogen atoms and R.sub.1 and R.sub.2 are not contemporaneously OY' or OY" groups respectively; m is an integer 1 or 2; n is an integer 3 to 8; p is an integer 2, 3, or 4; R.sub.3 is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl; R.sub.4 is a phenyl optionally substituted by halogen atom or a C.sub.1 -C.sub.3 alkyl or alkoxy group or a 5- or 6- membered heteroaryl containing one or more heteroatoms selected from oxygen, nitrogen and sulphur, optionally substituted by halogen atoms, hydroxy groups, C.sub.1 -C.sub.3 alkyl or alkoxy groups; X is CH.sub.2, NH, S, SO, SO.sub.2, CO, CF.sub.2, O and, when R.sub.4 is a 5- or 6- membered heteroaryl, X can be also a single bond. Pharmaceutically acceptable salts are described.
    Type: Grant
    Filed: April 30, 1996
    Date of Patent: May 5, 1998
    Assignee: Zambon Group, S.P.A.
    Inventors: Stefania Montanari, Paolo Cavalleri, Francesco Santangelo
  • Patent number: 5747516
    Abstract: Dihydroisoxazoles, dihydroisothiazoles, dihydropyrazoles, dihydrothiazoles and dihydroimidazoles of Formula I ##STR1## wherein: A is O; S; N; NR.sup.5 ; or CR.sup.14 ;G is C or N; provided that when G is C, A is O, S or NR.sup.5 and the floating double bond is attached to G; and when G is N, A is N or CR.sup.14 and the floating double bond is attached to A;W is O or S;X is OR.sup.1, S(O).sub.m R.sup.1 or halogen; andY, Z, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.14, and n are defined in the disclosure, are disclosed.Also disclosed are fungicidal compositions containing these compounds, and use of these cyclic amide compounds for controlling plant diseases caused by fungal plant pathogens.
    Type: Grant
    Filed: May 8, 1996
    Date of Patent: May 5, 1998
    Assignee: E. I. du Pont de Nemours and Company
    Inventors: Richard James Brown, King-Mo Sun, Deborah Ann Frasier
  • Patent number: 5723414
    Abstract: A class of 5-aryl-isoxazolinones and compositions thereof which are useful in the control of weeds is of the general formula ##STR1## wherein Ar is a substituted or unsubstituted aryl or heteroaryl;R.sup.2 is alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl or alkoxyalkyl, all of which may be substituted with one or more halogen atoms;R.sup.4 is alkynyl or alkoxyalkyl, both of which may be substituted with one or more halogen atoms; andX is an oxygen or a sulfur atom.
    Type: Grant
    Filed: January 21, 1997
    Date of Patent: March 3, 1998
    Assignee: Rohm and Haas Company
    Inventor: Colin Michael Tice
  • Patent number: 5705516
    Abstract: A compound having the formula R--S(O).sub.n CH.sub.2 CH.sub.2 CH.dbd.CF.sub.
    Type: Grant
    Filed: March 8, 1995
    Date of Patent: January 6, 1998
    Assignee: Zeneca Limited
    Inventors: Michael Drysdale Turnbull, Alison Mary Smith, Roger Salmon
  • Patent number: 5703065
    Abstract: The invention relates to compounds of the formula ##STR1## and to pharmaceutically acceptable salts thereof, wherein A, W, P, R.sup.3, Q and R.sup.1 are as defined herein. The compounds of formula I, and pharmaceutically acceptable salts thereof, are substance P antagonists and as such are useful in the treament of various inflammatory and central nervous system disorders.
    Type: Grant
    Filed: May 7, 1996
    Date of Patent: December 30, 1997
    Assignee: Pfizer Inc.
    Inventor: Harry R. Howard, Jr.
  • 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: 5686434
    Abstract: This invention relates to 3-aryl-2-isoxazoline compounds which are selective inhibitors of phosphodiesterase type IV (PDE.sub.IV). The 3-aryl-2-isoxazolines are useful in the treatment of AIDS, asthma, arthritis, bronchitis, chronic obstructive pulmonary disease, psoriasis, allergic rhinitis, dermatitis, shock, atopic dermatitis, rheumatoid arthritis and osteoarthritis. This invention also relates to pharmaceutical compositions useful therefor.
    Type: Grant
    Filed: May 15, 1996
    Date of Patent: November 11, 1997
    Assignee: Pfizer Inc.
    Inventor: Edward Fox Kleinman
  • Patent number: 5684198
    Abstract: Amides having formula I: ##STR1## wherein E, X, R.sup.2 and R.sup.3 have the meanings given in the specification, and pharmaceutically acceptable salts and pharmaceutically acceptable in vivo hydrolysable esters thereof,which are useful in the treatment of urinary incontinence. Further provided are processes for preparing the aides and pharmaceutical compositions containing them.
    Type: Grant
    Filed: August 23, 1996
    Date of Patent: November 4, 1997
    Assignee: Imperial Chemical Industries, PLC
    Inventors: Keith Russell, Cyrus John Ohnmacht, Keith Hopkinson Gibson
  • Patent number: 5674811
    Abstract: A cyanoketone derivatives of the following formula (1) ##STR1## which are characterized by excellent herbicidal activity and effectiveness against a variety of broad leafed weeds, including barnyard grass, green foxtail, velvet leaf, livid amaranth and hairy beggar ticks.
    Type: Grant
    Filed: October 6, 1994
    Date of Patent: October 7, 1997
    Assignee: Tokuyama Corporation
    Inventors: Toshio Kitajima, Tadashi Kobutani, Shozo Kato, Masao Yamaguchi, Masahiko Ishizaki, deceased
  • Patent number: 5674894
    Abstract: The current invention discloses novel amidine derivatives with nitric oxide donating property that can inhibit platelet aggregation and promote vasodilation in a single compound.
    Type: Grant
    Filed: May 15, 1995
    Date of Patent: October 7, 1997
    Assignee: G.D. Searle & Co.
    Inventors: Mark G. Currie, Foe S. Tjoeng, Mark E. Zupec
  • 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: 5643923
    Abstract: Compounds of formula (I): ##STR1## wherein R.sup.1 is hydrogen, halogen or alkyl; R.sup.2 is hydrogen, alkyl, optionally substituted phenyl or a heterocycle; or R.sup.1 and R.sup.2 together form a group of formula --CR.sup.4 .dbd.CR.sup.5 --CR.sup.6 .dbd.CR.sup.7 --, where R.sup.4, R.sup.5, R.sup.6 and R.sup.7 are hydrogen, halogen, alkyl group, alkoxy, halomethyl, alkylamino, dialkylamino, hydroxy, nitro, aliphatic carboxylic acylamino or amino; and R.sup.3 is piperidyl, substituted piperidyl or quinuclidinyl. The compounds are useful in the treatment and prophylaxis of cognitive disorders, notably senile dementia, including Alzheimer's disease. Processes for preparing the compounds are also provided.
    Type: Grant
    Filed: August 27, 1992
    Date of Patent: July 1, 1997
    Assignee: Sankyo Company, Limited
    Inventors: Mitsuo Nagano, Takeo Kobayashi, Junichi Sakai, Masao Kozuka, Nobuyoshi Iwata, Yoshiko Kubo
  • 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: 5629265
    Abstract: Disclosed herein are cyanoketone derivatives of the following formula (1) ##STR1## such as 1-cyano-1-piperidinocarbonyl-3-[4-(2-chloro-4-trifluoromethylphenoxy)pheno xy]-2-butanone, 1-cyano-1-piperidinocarbonyl-3-[4-(3-chloro-5-trifluoromethyl-2-pyridyloxy )phenoxy]-2-butanone, 1-cyano-1-(N-methyl-N-dichlorophenyl)aminocarbonyl-3-[4-(2-quinoxalyloxy)p henoxy]-2-butanone, 1-cyano-1-(N,N-dibutyl)aminocarbonyl-3-[4-(3-chloro-5-trifluoromethyl-2-py ridyloxy)phenoxy-2-butanone, and the like, which are characterized by excellent herbicidal activity and effectiveness against a variety of gramineous weeds.
    Type: Grant
    Filed: June 22, 1994
    Date of Patent: May 13, 1997
    Assignee: Tokuyama Corporation
    Inventors: Masahiko Ishizaki, Seiji Nagata, Junji Takenaka
  • Patent number: 5622971
    Abstract: A compound of the formula (I): ##STR1## or a pharmaceutically acceptable salt thereof is disclosed, as well as processes for and intermediates in the preparation thereof, and a method of antagonizing endothelin.
    Type: Grant
    Filed: June 1, 1995
    Date of Patent: April 22, 1997
    Assignee: Abbott Laboratories
    Inventors: Martin Winn, Steven A. Boyd, Charles W. Hutchins, Hwan-Soo Jae, Andrew S. Tasker, Thomas W. von Geldern, Jeffrey A. Kester, Bryan K. Sorensen
  • Patent number: 5621109
    Abstract: A retroviral protease inhibiting compound of the formula: ##STR1## is disclosed wherein the terms R.sub.1, R.sub.2, R.sub.5, R.sub.6, Y, Y', m and n are herein defined.
    Type: Grant
    Filed: May 31, 1995
    Date of Patent: April 15, 1997
    Assignee: Abbott Laboratories
    Inventors: Daniel W. Norbeck, Hing L. Sham, Dale J. Kempf, Chen Zhao
  • Patent number: 5618775
    Abstract: Mixtures of optically active cyclohexenone oxime ethers having R- and S-configuration in the oxime ether moiety of the formula I ##STR1## (R.sup.1 =C.sub.1 -C.sub.6 -alkyl; ##STR2## X=C.sub.1-C.sub.4 -alkyl, C.sub.1 -C.sub.4 -haloalkyl; m=0-3 or 1-4 where all X's are halogen;n=0-3 or 1-5 where all X's are halogen;R.sup.2 =C.sub.1 -C.sub.4 -alkoxy-C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.4 -alkylthio-C.sub.1 -C.sub.6 -alkyl, substituted or unsubstituted C.sub.3 -C.sub.7 -cycloalkyl, substituted or unsubstituted C.sub.5 -C.sub.7 -cycloalkenyl, substituted or unsubstituted 5-membered saturated heterocyclic structure, substituted or unsubstituted 6- or 7-membered heterocyclic structure, substituted or unsubstituted 5-membered heteroaromatic structure, substituted or unsubstituted phenyl or pyridyl)and their agriculturally useful salts and esters with C.sub.1 -C.sub.10 -carboxylic acids and inorganic acids.
    Type: Grant
    Filed: August 11, 1994
    Date of Patent: April 8, 1997
    Assignee: BASF Aktiengesellschaft
    Inventors: Ulf Misslitz, Norbert Meyer, Juergen Kast, Wolfgang Ladner, Helmut Walter, Karl-Otto Westphalen, Uwe Kardorff, Matthias Gerber
  • Patent number: 5599942
    Abstract: Taxoids having a 1,3-oxazole containing moiety at the 13-position of the taxane nucleus.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: February 4, 1997
    Assignee: Rhone-Poulenc Rorer S.A.
    Inventors: Herv e Bouchard, Jean-Dominique Bourzat, Alain Commercon