Chalcogen Bonded Directly To Ring Carbon Of The Oxazole Ring Patents (Class 548/243)
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Patent number: 6048885Abstract: 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: GrantFiled: August 21, 1996Date of Patent: April 11, 2000Assignee: Shionogi & Co., Ltd.Inventors: Akira Takase, Hiroyuki Kai, Kuniyoshi Nishida, Tsuneo Iwakawa, Kazuo Ueda, Michio Masuko
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Patent number: 6043377Abstract: 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: GrantFiled: December 8, 1998Date of Patent: March 28, 2000Assignee: Bayer AktiengesellschaftInventors: Lutz Assmann, Hans-Ludwig Elbe, Ralf Tiemann, Markus Heil, Klaus Stenzel
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Patent number: 6030970Abstract: Novel to isooxazoles, oxazoles, thiazoles, isothiazoles and imidazoles, pharmaceutical compositions containing these compounds and their use as endothelin receptor antagonists are described.Type: GrantFiled: February 2, 1998Date of Patent: February 29, 2000Assignee: Smithkline Beecham CorporationInventors: John Duncan Elliott, Juan Ignacio Luengo, Jia-Ning Xiang
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Patent number: 6025382Abstract: 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: GrantFiled: April 30, 1997Date of Patent: February 15, 2000Assignee: Eli Lilly and CompanyInventors: 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
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Patent number: 6022977Abstract: 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: GrantFiled: March 25, 1998Date of Patent: February 8, 2000Assignee: DuPont Pharmaceuticals CompanyInventors: Lin-Hua Zhang, Luigi Anzalone, Jaan A. Pesti, Jianguo Yin
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Patent number: 6020354Abstract: 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: GrantFiled: January 28, 1998Date of Patent: February 1, 2000Assignee: Bayer AktiengesellschaftInventors: Lutz Assmann, Albrecht Marhold, Ralf Tiemann, Klaus Stenzel
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Patent number: 6015909Abstract: 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: GrantFiled: September 3, 1997Date of Patent: January 18, 2000Assignee: Fuji Photo Film Co., Ltd.Inventors: Toshiki Fujiwara, Seiji Yamashita, Keiichi Suzuki
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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: 6004955Type: GrantFiled: August 12, 1998Date of Patent: December 21, 1999Assignee: DuPont Pharmaceuticals CompanyInventors: Fuqiang Jin, Pasquale Nicholas Confalone
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Patent number: 6005116Abstract: 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: GrantFiled: August 26, 1998Date of Patent: December 21, 1999Assignee: Sankyo Company, LimitedInventors: Koichi Kojima, Junichi Sakai, Naozumi Samata, Masao Kozuka, Kenji Yoshimi, Tsugio Kaneko
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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: 5985903Abstract: 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: GrantFiled: December 19, 1997Date of Patent: November 16, 1999Assignee: Bayer AktiengesellschaftInventors: Lutz Assmann, Ralf Tiemann, Martin Kugler, Heinrich Schrage, Klaus Stenzel
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Patent number: 5962490Abstract: 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: GrantFiled: September 27, 1996Date of Patent: October 5, 1999Assignee: Texas Biotechnology CorporationInventors: Ming Fai Chan, Chengde Wu, Bore Gowda Raju, Timothy Kogan, Adam Kois, Erik Joel Verner, Rosario Silvestre Castillo, Venkatachalapathi Yalamorri, Vitukudi Narayanaiyengar Balaji
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Patent number: 5959119Abstract: 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: GrantFiled: October 20, 1998Date of Patent: September 28, 1999Assignee: Bayer AktiengesellschaftInventors: Bernd Gallenkamp, Lothar Rohe
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Patent number: 5952354Abstract: 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: GrantFiled: July 21, 1993Date of Patent: September 14, 1999Assignee: American Home Products CorporationInventors: Thomas Joseph Commons, Donald Peter Strike, Christa Marie LaClair
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Patent number: 5939418Abstract: 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: GrantFiled: December 17, 1996Date of Patent: August 17, 1999Assignee: The DuPont Merck Pharmaceutical CompanyInventors: Mimi Lifen Quan, John Wityak, Robert Anthony Galemmo, Jr., Petrus F. W. Stouten, James Russell Pruitt, Donald J. P. Pinto
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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: 5932583Abstract: 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: GrantFiled: December 23, 1997Date of Patent: August 3, 1999Assignee: Novartis Crop Protection, Inc.Inventors: Hugo Ziegler, Stephan Trah, Rene Zurfluh, Anthony Cornelius O'Sullivan
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Patent number: 5932731Abstract: 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: GrantFiled: December 22, 1997Date of Patent: August 3, 1999Assignee: Sumitomo Seika Chemicals Co., Ltd.Inventors: Hiroshi Goda, Mikio Yamamoto, Jun-ichi Sakamoto, Hitoshi Karino
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Patent number: 5929279Abstract: 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: GrantFiled: October 7, 1997Date of Patent: July 27, 1999Assignee: BASF AktiengesellschaftInventors: Ruth Muller, Remy Benoit, Herbert Bayer, Norbert Gotz, Hubert Sauter
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Patent number: 5925663Abstract: 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: GrantFiled: October 3, 1997Date of Patent: July 20, 1999Assignee: Bayer AktiengesellschaftInventors: Lutz Assmann, Albrecht Marhold, Klaus Stenzel, Martin Kugler
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Patent number: 5919944Abstract: 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: GrantFiled: July 20, 1998Date of Patent: July 6, 1999Assignee: Ciba Specialty Chemicals CorporationInventor: Sameer Eldin
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Patent number: 5863865Abstract: This invention relates to 4-benzoylisoxazoles of formula (I) ##STR1## as well as herbicide compositions containing them and their use as herbicides.Type: GrantFiled: October 28, 1997Date of Patent: January 26, 1999Assignee: Zeneca LimitedInventors: David L. Lee, Nigel Barnes
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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: 5852007Abstract: 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: GrantFiled: February 6, 1997Date of Patent: December 22, 1998Assignee: Cephalon, Inc.Inventor: Sankar Chatterjee
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Patent number: 5834508Abstract: 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: GrantFiled: February 6, 1997Date of Patent: November 10, 1998Assignee: Mitsubishi Chemical CorporationInventors: Ryoichi Ando, Naoko Ando, Hirokazu Masuda, Yasuhiro Morinaka, Chizuko Takahashi, Yoshikuni Tamao, Akihiro Tobe
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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: 5824677Abstract: 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: GrantFiled: June 7, 1995Date of Patent: October 20, 1998Assignee: Cell Therapeutics, Inc.Inventors: J. Peter Klein, Gail E. Underiner, Anil M. Kumar
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Patent number: 5811441Abstract: 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: GrantFiled: September 3, 1997Date of Patent: September 22, 1998Assignee: The DuPont Merck Pharmaceutical CompanyInventors: Richard Eric Olson, John Wityak
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Patent number: 5760059Abstract: 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: GrantFiled: March 29, 1996Date of Patent: June 2, 1998Assignee: Glaxo Wellcome SpAInventors: Alfredo Cugola, Romano DiFabio, Giorgio Pentassuglia
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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: 5747513Abstract: 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: GrantFiled: April 30, 1996Date of Patent: May 5, 1998Assignee: Zambon Group, S.P.A.Inventors: Stefania Montanari, Paolo Cavalleri, Francesco Santangelo
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Patent number: 5747516Abstract: 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: GrantFiled: May 8, 1996Date of Patent: May 5, 1998Assignee: E. I. du Pont de Nemours and CompanyInventors: Richard James Brown, King-Mo Sun, Deborah Ann Frasier
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Patent number: 5723414Abstract: 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: GrantFiled: January 21, 1997Date of Patent: March 3, 1998Assignee: Rohm and Haas CompanyInventor: Colin Michael Tice
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Patent number: 5705516Abstract: A compound having the formula R--S(O).sub.n CH.sub.2 CH.sub.2 CH.dbd.CF.sub.Type: GrantFiled: March 8, 1995Date of Patent: January 6, 1998Assignee: Zeneca LimitedInventors: Michael Drysdale Turnbull, Alison Mary Smith, Roger Salmon
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Patent number: 5703065Abstract: 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: GrantFiled: May 7, 1996Date of Patent: December 30, 1997Assignee: Pfizer Inc.Inventor: Harry R. Howard, Jr.
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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: 5686434Abstract: 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: GrantFiled: May 15, 1996Date of Patent: November 11, 1997Assignee: Pfizer Inc.Inventor: Edward Fox Kleinman
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Patent number: 5684198Abstract: 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: GrantFiled: August 23, 1996Date of Patent: November 4, 1997Assignee: Imperial Chemical Industries, PLCInventors: Keith Russell, Cyrus John Ohnmacht, Keith Hopkinson Gibson
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Patent number: 5674811Abstract: 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: GrantFiled: October 6, 1994Date of Patent: October 7, 1997Assignee: Tokuyama CorporationInventors: Toshio Kitajima, Tadashi Kobutani, Shozo Kato, Masao Yamaguchi, Masahiko Ishizaki, deceased
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Patent number: 5674894Abstract: 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: GrantFiled: May 15, 1995Date of Patent: October 7, 1997Assignee: G.D. Searle & Co.Inventors: Mark G. Currie, Foe S. Tjoeng, Mark E. Zupec
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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: 5643923Abstract: 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: GrantFiled: August 27, 1992Date of Patent: July 1, 1997Assignee: Sankyo Company, LimitedInventors: Mitsuo Nagano, Takeo Kobayashi, Junichi Sakai, Masao Kozuka, Nobuyoshi Iwata, Yoshiko Kubo
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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: 5629265Abstract: 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: GrantFiled: June 22, 1994Date of Patent: May 13, 1997Assignee: Tokuyama CorporationInventors: Masahiko Ishizaki, Seiji Nagata, Junji Takenaka
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Patent number: 5622971Abstract: 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: GrantFiled: June 1, 1995Date of Patent: April 22, 1997Assignee: Abbott LaboratoriesInventors: Martin Winn, Steven A. Boyd, Charles W. Hutchins, Hwan-Soo Jae, Andrew S. Tasker, Thomas W. von Geldern, Jeffrey A. Kester, Bryan K. Sorensen
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Patent number: 5621109Abstract: 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: GrantFiled: May 31, 1995Date of Patent: April 15, 1997Assignee: Abbott LaboratoriesInventors: Daniel W. Norbeck, Hing L. Sham, Dale J. Kempf, Chen Zhao
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Patent number: 5618775Abstract: 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: GrantFiled: August 11, 1994Date of Patent: April 8, 1997Assignee: BASF AktiengesellschaftInventors: Ulf Misslitz, Norbert Meyer, Juergen Kast, Wolfgang Ladner, Helmut Walter, Karl-Otto Westphalen, Uwe Kardorff, Matthias Gerber
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Patent number: 5599942Abstract: Taxoids having a 1,3-oxazole containing moiety at the 13-position of the taxane nucleus.Type: GrantFiled: June 7, 1995Date of Patent: February 4, 1997Assignee: Rhone-Poulenc Rorer S.A.Inventors: Herv e Bouchard, Jean-Dominique Bourzat, Alain Commercon