Chalcogen Bonded Directly To Ring Carbon Of The Oxazole Ring Patents (Class 548/243)
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Patent number: 5208333Abstract: (2R)-1-(Aryloxy)-3-(butyryloxy)-2-propanols of the general formula (I), ##STR1## where Ar is a monocyclic or polycyclic aromatic or heteroaromatic radical, and a process for their preparation by the reaction of (2R)-glycidyl butyrate with an aromatic hydroxy compound Ar--OH in the presence of a quaternary ammonium halide.Type: GrantFiled: December 9, 1988Date of Patent: May 4, 1993Assignee: BASF AktiengesellschaftInventors: Axel Paul, Wolfgang Ladner, Hardo Siegel
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Patent number: 5208251Abstract: The present invention is 3,5-substituted, isoxazoles, pyrazoles, isothiazoles, and analogs thereof having 5-lipoxygenase or cyclooxygenase inhibiting activity or as a sunscreen.Type: GrantFiled: August 16, 1989Date of Patent: May 4, 1993Assignee: Warner-Lambert CompanyInventors: Thomas R. Belliotti, David T. Connor, Daniel L. Flynn, Catherine R. Kostlan, Donald E. Nies
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Patent number: 5204374Abstract: New cycloalkano[b]dihydroindoles and -indolesulphonamides, substituted by heterocycles, of the formula (I) ##STR1## in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are identical or different andrepresent hydrogen, nitro, cyano, halogen, trifluoromethyl, carboxyl, hydroxyl or trifluoromethoxy, orrepresent a group of the formula --S(O).sub.w R.sup.5, in whichR.sup.5 denotes alkyl or optionally substituted aryl,w denotes the number 0, 1 or 2, orrepresents alkoxy or alkoxycarbonyl, or benzyloxy, orrepresents a group of the formula --NR.sup.6 R.sup.7, in whichR.sup.6 and R.sup.7 are identical or different anddenote hydrogen, alkyl or acyl ordenote aryl, ordenote a group of the formula --S(O).sub.w R.sup.5, in which R.sup.Type: GrantFiled: April 3, 1991Date of Patent: April 20, 1993Assignee: Bayer AktiengesellschaftInventors: Ulrich E. Muller, Ulrich Rosentreter, Ulrich Niewohner, Elisabeth Perzborn, Erwin Bischoff, Hans-Georg Dellweg, Peter Norman, Nigel J. Cuthbert, Hilary P. Francis
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Patent number: 5201935Abstract: Cyclohexenone derivatives of the general formula I ##STR1## where the substituents have the following meanings: R.sup.1 substituted or unsubstituted C.sub.1 -C.sub.6 -alkyl, C.sub.3 -C.sub.6 -alkenyl or C.sub.3 -C.sub.6 -alkynyl, phenyl, benzyl or thenyl;R.sup.2 substituted or unsubstituted C.sub.1 -C.sub.6 -alkyl, C.sub.3 -C.sub.6 -alkenyl, C.sub.3 -C.sub.6 -alkynyl or phenyl;R.sup.3 hydrogen, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.10 -alkylcarbonyl, C.sub.1 -C.sub.6 -alkylsulfonyl, C.sub.1 -C.sub.4 -trialkylsilyl, C.sub.1 -C.sub.4 -dialkylphosphonyl, C.sub.1 -C.sub.4 -dialkylthiophosphonyl, C.sub.3 -C.sub.6 -alkenyl, C.sub.3 -C.sub.6 -alkenylcarbonyl, C.sub.3 -C.sub.6 -alkynyl orsubstituted or unsubstituted benzoyl- or phenylsulfonyl;R.sup.4 hydrogen, cyano, halogen, C.sub.1 -C.sub.6 -alkyl or C.sub.1 -C.sub.6 -alkoxycarbonyl;A a substituted or unsubstituted C.sub.1 -C.sub.Type: GrantFiled: August 26, 1992Date of Patent: April 13, 1993Assignee: BASF AktiengesellschaftInventors: Dieter Kolassa, Juergen Kasi, Thomas Kuekenhoehner, Norbert Meyer, Karl-Otto Westphalen, Bruno Wuerzer
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Patent number: 5196541Abstract: There is described a new process for the preparation of substituted 3-aminoacrylic esters of the general formula (I) ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, X and n have the meaning given in the description.The 3-aminoacrylic esters of the formula (I) are obtained by reacting acetic esters of the formula (II)R.sup.1 --(X).sub.n --CH.sub.2 --COOR.sup.Type: GrantFiled: August 2, 1991Date of Patent: March 23, 1993Assignee: Bayer AktiengesellschaftInventors: Herbert Gayer, Alexander Klausener, Peter C. Knuppel, Fritz Maurer
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Patent number: 5190963Abstract: Cyclopropane(thio)carboxamides of the general formula I ##STR1## where the index and the substituents have the following meanings: n is 0, 1 or 2, it being possible for the R.sup.2 radicals to be different when n is 2;A.sup.1 and A.sup.2 are substituted or unsubstituted alkylene;R.sup.1 is hydrogen, halogen or alkyl;R.sup.2 is halogen or alkyl;X is substituted or unsubstituted 5-membered heteroaryl, substituted or unsubstituted pyrazolyl-1-oxy or triazolyl-1-oxy; andY is oxygen or sulfur,processes for their manufacture, intermediates therefor, and the use of compounds I.Type: GrantFiled: February 3, 1992Date of Patent: March 2, 1993Assignee: BASF AktiengesellschaftInventors: Christoph Nuebling, Hans Theobald, Uwe Kardorff, Wolfgang Krieg, Christoph Kuenast
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Patent number: 5177207Abstract: Novel forskolin derivatives, intermediates and processes for the preparation thereof, and methods for treating cardiac failure and memory deficit utilizing compounds or compositions thereof are disclosed.Type: GrantFiled: November 21, 1990Date of Patent: January 5, 1993Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Raymond W. Kosley, Jr., Gerard O'Malley, Bettina Spahl
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Patent number: 5158598Abstract: Bithienyl derivatives of the formula Ia ##STR1## where the substituents have the following meanings: R.sup.1, R.sup.2 hydrogen, halogen, nitro, formyl, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -haloalkyl, C.sub.3 -C.sub.8 -cycloalkyl, C.sub.3 -C.sub.8 -cycloalkoxy, C.sub.1 -C.sub.6 -alkoxy, C.sub.1 -C.sub.4 -haloalkoxy, C.sub.1 -C.sub.4 -alkylthio, C.sub.1 -C.sub.4 -haloalkylthio, substituted or unsubstituted C.sub.1 -C.sub.6 -alkylcarbonyl, substituted or unsubstituted C.sub.3 -C.sub.6 -cycloalkylcarbonyl, substituted or unsubstituted C.sub.1 -C.sub.6 -alkoxycarbonyl and/or phenylcarbonyl;R.sup.3 hydrogen, halogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -alkylthio, C.sub.1 -C.sub.4 -haloalkyl or C.sub.1 -C.sub.4 -haloalkoxy;A --CSNH.sub.Type: GrantFiled: August 4, 1989Date of Patent: October 27, 1992Assignee: BASF AktiengesellschaftInventors: Reiner Kober, Joachim Leyendecker, Rainer Seele, Klaus Fischer, Hans Theobald, Bruno Wuerzer, Karl-Otto Westphalen, Norbert Meyer
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Patent number: 5151441Abstract: 3-Isoxazolylbenzyl esters of the general formulae Ia and Ib ##STR1## where R is halogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -haloalkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -haloalkoxy, C.sub.2 --C.sub.4 -alkenyl, C.sub.2 -C.sub.4 -haloalkenyl, C.sub.2 -C.sub.4 -alkynyl, C.sub.2 -C.sub.4 -haloalkynyl, unsubstituted or substituted phenylethenyl, C.sub.3 -C.sub.8 -cycloalkyl, aryl, hetaryl, CO.sub.2 R.sup.3 or CONR.sup.4 R.sup.5,R.sup.3, R.sup.4 and R.sup.5 are each hydrogen or C.sub.1 -C.sub.6 -alkyl,n is 0, 1 or 2, and the radicals R may be different when n is 2,R.sup.1 is halogen or C.sub.1 -C.sub.4 -alkyl,R.sup.2 is hydrogen, C.sub.1 -C.sub.4 -alkyl, C.sub.2 -C.sub.4 -alkenyl, C.sub.2 -C.sub.4 -alkynyl or cyano andA is the carbonyl radical of an acid component usually found in pyrethroids, are contained in pesticides.Type: GrantFiled: May 14, 1991Date of Patent: September 29, 1992Assignee: BASF AktiengesellschaftInventors: Stefan Mueller, Hans Theobald, Bernd Wolf, Peter Hofmeister, Uwe Kardorff, Christoph Kuenast
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Patent number: 5138067Abstract: Lipid derivatives represented by the formula: ##STR1## wherein R.sub.1 is alkyl or alkylcarbamoyl; R.sub.2 is lower alkyloxy, lower alkylcarbamoyloxy, lower alkylcarbonylamino, lower alkyloxycarbonylamino, lower alkylureido, lower alkyloxymethyl, lower alkylcarbonylmethyl, cyanomethyl, heterocyclic group, or heterocyclyloxy; R.sub.2 ' is hydrogen or R.sub.2 and R.sub.2 ' taken together with R.sub.2 form --O(CH.sub.2).sub.m -- wherein m is an integer of 1 to 5; R.sub.3, R.sub.4, and R.sub.5 each is hydrogen or lower alkyl or two or three of R.sub.3, R.sub.4, and R.sub.5 taken together with the adjacent nitrogen atom form cyclic ammonio; R.sub.6 is hydrogen or lower alkylcarbonyl; X.sup.- is a counter anion; Y is oxygen or sulfur; and n is an integer of 1 to 10, being useful as PAF antagonists, e.g., as antithrombotic, antivasoconstricting, antibronchoconstricting agent or antitumor agent.Type: GrantFiled: May 29, 1991Date of Patent: August 11, 1992Assignee: Shionogi & Co. Ltd.Inventors: Susumu Kamata, Tatsuo Tsuri, Nobuhiro Haga, Takeaki Matsui, Morio Kishi, Kimio Takahashi, Sanji Hagishita, Kaoru Seno
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Patent number: 5128346Abstract: A compound of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are substituents; R.sub.6 is hydrogen, loweralkyl, cycloalkyl, loweralkenyl, arylalkyl, (substituted aryl)alkyl, or (heterocyclic)alkyl; B is a bond, an alkylene group, an alkenylene group, an alkadienylene group or a heteroatom containing linking group; D is a substituted acyl group or tetrazolyl; Z is CO, C(S) or S(O).sub.2 ; Ar is a heterocyclic group; and n is 1 to 3.Also disclosed are a composition and a method for antagonizing CCK, a composition and method for treating or preventing gastrointestinal, central nervous, appetite regulating and pain regulating systems, a composition and method for treating or preventing hyperinsulinemia, methods of making the compounds and intermediates useful in making the compounds.Type: GrantFiled: August 23, 1990Date of Patent: July 7, 1992Assignee: Abbott LaboratoriesInventors: Alex M. Nadzan, James F. Kerwin, Chun W. Lin
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Patent number: 5110986Abstract: This application relates to a process for preparing a N-t-alkyl-1,2-diacylhydrazine by reacting a 1,3,4-oxadiazole with a tertiary alkyl cation precursor in the presence of a strong acid catalyst. Preferably, the 1,3,4-oxadiazole is a 2,5-disubstituted-1,3,4-oxadiazole and more preferably a 2,5-diaryl-1,3,4-oxadiazole. The strong acid catalyst is preferably a sulfur containing acid and more preferably sulfuric acid.Type: GrantFiled: April 26, 1988Date of Patent: May 5, 1992Assignee: Rohm and Haas CompanyInventor: Martha J. Kelly
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Patent number: 5103007Abstract: Lipid derivatives represented by the formula: ##STR1## wherein R.sup.1 stands for an optionally substituted higher alkyl group, R.sup.2 stands for an optionally substituted lower alkyl group or an optionally substituted nitrogen-containing heterocyclic group, R.sup.3 stands for a tertiary amino group or a quaternary ammonium group, J stands for oxygen atom or S(O)t (where t deontes 0, 1 or 2), m and n respectively denotes 1 or 2, p denotes 0, 1 or 2, q and r respectively denote an integer of 2 to 5.and salts thereof have antitumor activities including differentiation-inducing activity and are useful as antitumor agents.Type: GrantFiled: October 27, 1989Date of Patent: April 7, 1992Assignee: Takeda Chemical Industries, Ltd.Inventors: Hiroaki Nomura, Hiroshi Akimoto, Keizo Inoue
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Patent number: 5098462Abstract: Substituted semicarbazones, thiosemicarbazones and isothiosemicarbazones and salts thereof, intermediates therefor, synthesis thereof, and the use of said compounds for the control of weeds.Type: GrantFiled: May 23, 1988Date of Patent: March 24, 1992Assignee: Sandoz Ltd.Inventors: Richard J. Anderson, Michael M. Leippe, Joe T. Bamberg
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Patent number: 5082947Abstract: A novel compound useful as an intermediate for synthesizing pesticides and medicine of the formula: ##STR1## in which: R is perfluoroalkyl, R.sup.1 is hydrogen, alkyl or optionally substituted phenyl, or a salt thereof.Type: GrantFiled: June 19, 1990Date of Patent: January 21, 1992Assignee: Shionogi & Co., Ltd.Inventors: Shinzaburo Sumimoto, Ichiro Ishizuka, Shiro Ueda, Hiroyuki Kai
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Patent number: 5081245Abstract: A compound represented by the formula: ##STR1## wherein R represents a hydrogen atom or a lower alkyl group;R.sup.1 represents a higher alkyl group which may be substituted;R.sup.2 represents a hydrogen atom or a lower alkyl group, a lower alkanoyl group or a nitrogen-containing 5- to 7-membered heterocyclic group each of which may be substituted; X represents a divalent group represented by the formula:--(OCH.sub.2 CH.sub.2).sub.p --wherein p represents an integer of 1 to 5, a divalent group represented by the formula:--O(CH.sub.2).sub.q --wherein q represents an integer of 3 to 8, or a divalent group represented by the formula:--(OCH.sub.2 CH.sub.2).sub.p --J--(CH.sub.2).sub.q --wherein J represents an oxygen atom or a group represented by the formula: --S(O).sub.Type: GrantFiled: August 18, 1989Date of Patent: January 14, 1992Assignee: Takeda Chemical Industries, Ltd.Inventors: Hiroaki Nomura, Hiroshi Akimoto, Eiko Imamiya, Keizo Inoue
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Patent number: 5080708Abstract: Isoxazole(isothiazole)-5-carboxamides of the formula ##STR1## where X is oxygen or sulfur,R.sup.1 is hydrogen, substituted or unsubstituted alkyl, alkoxy, substituted or unsubstituted cycloalkyl, a 5- or 6-membered heterocyclic radical having one or two heteroatoms selected from the group consisting of oxygen, sulfur and nitrogen, and which may be substituted, or substituted or unsubstituted phenyl, orR.sup.2 is formyl, 4,5-dihydrooxazol-2-yl or a radical of the formula COYR.sup.5 or CONR.sup.6 R.sup.7, whereY is oxygen or sulfur,R.sup.5 ishydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, haloalkenyl, substituted or unsubstituted alkynyl,cycloalkyl,cycloalkenyl,substituted or unsubstituted phenyl,a 5- or 6-membered heterocyclic radical having one or two heteroatoms selected from the group consisting of oxygen, sulfur and nitrogen,cycloalkanimino, phthalimido, succinimido, or a radical ##STR2## R.sup.3 and R.sup.Type: GrantFiled: April 13, 1989Date of Patent: January 14, 1992Assignee: BASF AktiengesellschaftInventors: Wolfgang Freund, Thomas Kuekenhoehner, Gerhard Hamprecht, Bruno Wuerzer, Karl-Otto Westphalen, Norbert Meyer, Hans Theobald
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Patent number: 5071994Abstract: 2-aryl-4-halomethyl-4-isoxazolin-3-1-derivatives of formula (I), useful as intermediates for positive working compounds in silver halide photographic materials ##STR1## wherein R.sup.1 represents a substituted or unsubstituted alkyl having from 1 to 6 carbon atoms or a substituted or unsubstituted aryl having from 6 to 24 carbon atoms; R.sup.2, R.sup.3, and R.sup.4, are the same or different, each having up to 20 carbon atoms and each represents hydrogen, a substituted or unsubstituted alkoxy, a substituted or unsubstituted aryloxy, a substituted or unsubstituted acyl, a substituted or unsubstituted alkoxycarbonyl, a substituted or unsubstituted aryloxycarbonyl, halogen, nitro, a substituted or unsubstituted carbamoyl, a substituted or unsubstituted sulfamoyl, a substituted or unsubstituted sulfonyl, cyano, trifluoromethyl, or carboxyl, with the proviso that at least one of said R.sup.2 and R.sup.Type: GrantFiled: January 23, 1991Date of Patent: December 10, 1991Assignee: Fuji Photo Film Co., Ltd.Inventors: Koki Nakamura, Shigeru Nakamura
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Patent number: 5066665Abstract: Substituted isoxazolidin-3-ones and derivatives thereof are described, as well as methods for the preparation and pharmaceutical compositions of same, which are useful as centrally acting muscarinic agents and are useful as analgesic agents for the treatment of pain, as sleep aids and as agents for treating the symptoms of senile dementia, Alzheimer's disease, Huntington's chorea, tardive dyskinesia, hyperkinesia, mania, or similar conditions of cerebral insufficiency characterized by decreased cerebral acetylcholine production or release.Type: GrantFiled: May 21, 1990Date of Patent: November 19, 1991Assignee: Warner-Lambert Co.Inventor: Sheila H. Hobbs
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Patent number: 5064847Abstract: There are described new 5-substituted 3-arylisoxazole derivatives of general formula I ##STR1## in which in which R.sub.1 and R.sub.2 have the meanings given in the description, processes for their preparation and their use as pesticides, especially against nematodes.Type: GrantFiled: May 1, 1990Date of Patent: November 12, 1991Assignee: Schering AktiengesellschaftInventors: Dieter Hubl, Ernst Pieroh
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Patent number: 5059614Abstract: The object of the invention are anticonvulsant heterocyclic compounds of general formula: ##STR1## in which R.sub.1 and R.sub.2 is each selected from C.sub.1 -C.sub.4 alkyl, phenyl, benzyl, trifluoromethyl or halogen, R.sub.3 is selected from hydrogen, hydroxy, C.sub.1 -C.sub.4 alkyl or alkoxy, R.sub.4, in position 3 or 5, is selected from hydrogen, trifluoromethyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkyl, or C.sub.1 -C.sub.4 hydroxyalkyl,R.sub.5 is selected from hydrogen or C.sub.4 -C.sub.4 alkyl or R.sub.4 and R.sub.5 together form a tetramethylene group, Z at position 3 or 5 on the heterocycle is selected from:--N(R.sub.6)--CO--, --CO--N(R.sub.6)--, --N(R.sub.6)--CO--N(R.sub.6)----CH(R.sub.6)--NH--CO--, or --NH-CO--CH(R.sub.6),in which R.sub.6 is selected from hydrogen or C.sub.1 -C.sub.4 alkyl.Type: GrantFiled: November 29, 1989Date of Patent: October 22, 1991Assignee: NovapharmeInventors: Francis Lepage, Bernard Hublot
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Patent number: 5059709Abstract: A novel process for producing .alpha.-[(dialkylamino) substituted-methylene].beta.-oxo-(substituted) propanenitriles of the formula: ##STR1## where R, R.sub.1 and R .sub.2 are defined in the specification by reacting a substituted isoxazole with a diaklylamide dimethylacetal is provided.Type: GrantFiled: November 13, 1990Date of Patent: October 22, 1991Assignee: American Cyanamid CompanyInventors: John P. Dusza, Robert F. Church
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Patent number: 5047554Abstract: This invention relates to novel 3-substituted-2-oxindole derivatives which are inhibitors of prostaglandin H.sub.2 synthase, 5-lipoxygenase and interleukin-1 biosynthesis. The compounds of the invention are useful as inhibitors of prostaglandin H.sub.2 synthase and interleukin-1 biosynthesis, per se, and as analgesic, antiinflammatory and antiarthritic agents in the treatment of chronic inflammatory diseases. This invention also relates to pharmaceutical compositions comprising said 3-substituted-2-oxindole derivatives; to methods of inhibiting prostaglandin H.sub.2 synthase and biosynthesis of interleukin-1; and to treating chronic inflammatory diseases in a mammal with said compounds. Further, this invention relates to certain novel carboxylic acids useful as intermediates in the preparation of the 3-substituted-2-oxindole derivatives of this invention and to a process for the preparation of the 3-substituted-2-oxindole derivatives.Type: GrantFiled: January 31, 1990Date of Patent: September 10, 1991Assignee: Pfizer Inc.Inventors: Frederick J. Ehrgott, Carl J. Goddard, Gary R. Schulte
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Patent number: 5043454Abstract: 1-Aryl- and 1-hetarylimidazolecarboxylic esters of the general formulae Ia and Ib ##STR1## where R.sup.1 is halogen or substituted or unsubstituted C.sub.1 -C.sub.4 -alkyl;R.sup.2 is substituted or unsubstituted C.sub.1 -C.sub.6 -alkyl; C.sub.3 -C.sub.6 -alkenyl, C.sub.3 -C.sub.6 -alkynyl or C.sub.3 -C.sub.6 -cycloalkyl;R.sup.3 is hydrogen or C.sub.1 -C.sub.4 -alkyl;R.sup.4 is substituted or unsubstituted phenyl or 5- or 6-membered heteroaromatic,processes for their manufacture, and agents containing them.Type: GrantFiled: January 9, 1990Date of Patent: August 27, 1991Assignee: BASF AktiengesellschaftInventors: Ulrich Wriede, Gerhard Hamprecht, Hermann Koehler, Bruno Wuerzer
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Patent number: 5041545Abstract: Hydrazide functionalized 2-hydroxybenzophenone ultraviolet light and heat stabilizers and derivatives are disclosed having the general formula: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, X, Y, Z, all substituents thereof, and n are set forth in the Summary of the Invention. Y--N(R.sup.6)--Z is the hydrazide or derivative group and --X--R.sup.5 -- links the hydrazide group to an aromatic nucleus of the optionally substituted benzophenone group. Derivatives are, for example, acyl hydrazides, diacyl hydrazides (including imides), hydrazones and alkyl hydrazides. The compounds are useful as ultraviolet light absorbers and heat stabilizers for plastics.Type: GrantFiled: April 6, 1989Date of Patent: August 20, 1991Assignee: Atochem North America, Inc.Inventor: Terry N. Myers
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Patent number: 5037841Abstract: Novel 1,3-disubstituted pyrrolidines active on the central nervous system of the formula ##STR1## wherein A denotes phenyl or hetaryl, which is optionally fused with aromatic, saturated or unsaturated cyclic or heterocyclic hydrocarbons, where this radical can optionally be substituted,X denotes --O--CH.sub.2 --, --CH.sub.2 --O-- or --O--,n denotes a number from 1 to 19, andB denotes cyano or a group of the formula --COOR.sup.1, --CONR.sup.2 R.sup.3, --SO.sub.2 NR.sup.2 R.sup.3, --SO.sub.m R.sup.4, --NR.sup.5 R.sup.6, or --C.tbd.C--CH.sub.2 --NR.sup.5 R.sup.6,and salts thereof.Type: GrantFiled: April 12, 1989Date of Patent: August 6, 1991Assignee: Bayer AktiengesellschaftInventors: Rudolf Schohe, Peter-Rudolf Seidel, Jorg Traber, Thomas Glaser
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Patent number: 5021438Abstract: Novel compounds having an affinity for 5-hydroxytryptamine receptors of the formula ##STR1## in which R.sup.1 stands for H, alkyl, aralkyl or heteroarylalkyl,X stands for H, OCH.sub.3, OH, SCH.sub.3, halogen, CN or CONH.sub.2,Y stands for a straight-chain or branched, saturated or unsaturated alkylene chain having up to 6 carbon atomsandZ stands for a group of the formula ##STR2## --OR.sup.4, --SO.sub.m R.sup.5, --COOR.sup.6 or CONR.sup.7 R.sup.8 or salts thereof.Type: GrantFiled: March 15, 1989Date of Patent: June 4, 1991Assignee: Bayer AktiengesellschaftInventors: Bodo Junge, Bernd Richter, Thomas Glaser, Jorg Traber
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Patent number: 5021439Abstract: A compound having the formula (I) or (II) ##STR1## wherein R.sup.1 is a hydrogen atom or an organic residue bonded via a carbon atom, R.sup.2 is a hydrogen atom or a N-protecting group, --COR.sup.3 is an optionally esterified or amidated carboxyl group, R.sup.4 and R.sup.5 are the same or different and respectively a hydrogen atom or an acyl group or a chain or alicyclic hydrocarbon group optionally having an aryl substituent, R.sup.6 is NOH or O, n is an integer of 0 to 3, or R.sup.4 and R.sup.5 together with the adjacent nitrogen atom may form a ring or an optionally substituted benzylidene amino group, which is useful therapeutics of brain dysfunction.Type: GrantFiled: September 18, 1989Date of Patent: June 4, 1991Assignee: Takeda Chemical Industries, Ltd.Inventors: Setsuo Harada, Akinobu Nagaoka, Katsumi Itoh, Shinji Terao
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Patent number: 5012000Abstract: A method for the preparation of chiral 2-amino-1,3-diols is disclosed. The method involves four steps including performance of an aldol condensation with a chiral oxazolidinone on an aldehyde, treating the aldol condensation product with an alkali metal azide, treating the product with a borohydride reagent and reducing the azide to an amine.Type: GrantFiled: October 30, 1989Date of Patent: April 30, 1991Assignee: Eastman Kodak CompanyInventors: Carl R. Illig, Alexander L. Weis
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Patent number: 4987146Abstract: N-hetaryl imidazole derivatives of general Formula I ##STR1##are disclosed in whichHet represents an optionally substituted monocyclic or bicyclic heteroaromate,R.sup.3 represents hydrogen, a straight or branched C.sub.1-6 -alkyl group, or a C.sub.1-6 -alkoxy-alkyl group, andR.sup.4 represents --COOR.sup.5 --CONR.sup.6 R.sup.7 --CN, ##STR2##with R.sup.5 meaning hydrogen, a straight or branched C.sub.1-6 -alkyl group, R.sup.6 and R.sup.7 are the same of different and represent hydrogen or a straight, branched, or cyclic alkyl group with up to 7 carbon atoms or, together with the nitrogen atom, form a saturated five or six ring optionally containing another heteroatom and R.sup.8 means hydrogen or a straight, branched or cyclic alkyl group with up to 7 carbon atoms.Type: GrantFiled: July 14, 1989Date of Patent: January 22, 1991Assignee: Schering AktiengesellschaftInventors: Ralph Rohde, Helmut Biere, Ralph Schmiechen, John S. Andrews, David N. Stephens
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Patent number: 4985428Abstract: Nootropically active isoxazoles which are certain specified derivatives of N-(5-isoxazolecarbonyl)-4 aminobutyric acid.Type: GrantFiled: March 20, 1989Date of Patent: January 15, 1991Assignee: Zambon Group S.p.A.Inventors: Angelo Carenzi, Dario Chiarino, Davide Della Bella, Mauro Napoletano, Alberto Sala
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Patent number: 4968681Abstract: Substituted hydroxylamines of the formula ##STR1## in which R.sup.1 stands for an aromatic or heterocyclic radical, are especially useful in the treatment of hyperlipoproteinaemia, lipoproteinaemia and atherosclerosis.Type: GrantFiled: November 15, 1988Date of Patent: November 6, 1990Assignee: Bayer AktiengesellschaftInventors: Walter Hubsch, Rolf Angerbauer, Peter Fey, Hilmar Bischoff, Dieter Petzinna, Delf Schmidt
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Patent number: 4954518Abstract: This invention relates to a 4H-1-benzopyran-4-one derivative represented by the formula: ##STR1## or a salt thereof, a process for producing the same and a pharmaceutical composition comprising the same as active ingredient.Type: GrantFiled: October 7, 1988Date of Patent: September 4, 1990Assignee: Toyama Chemical Company, Ltd.Inventors: Shuntaro Takano, Chosaku Yoshida, Takihiro Inaba, Keiichi Tanaka, Ryuko Takeno, Hideyoshi Nagaki, Tomoya Shimotori, Shinji Makino
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Patent number: 4952700Abstract: A process for forming isoxazolines or isoxazoles by contacting, in the presence of base, a nitro compound, a cyclic anhydride and a dipolarophile. The dicarboxylic acid is readily regenerated to be again reused as the dehydrating agent of additional nitro compound.Type: GrantFiled: April 25, 1988Date of Patent: August 28, 1990Assignee: W.R. Grace & Co.-Conn.Inventors: Sheldon B. Markofsky, Steven A. Kothe
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Patent number: 4946963Abstract: An isoxazolidin-3,5-dione for the control of hyperlipidemia in mammals having the following structural formula: ##STR1## wherein R.sup.1 and R.sup.2 are each an alkyl of 1 to 4 carbons; R.sup.3 is an alkoxybenzoyl group containing from 1 to 3 alkoxy groups wherein the alkoxy groups have from 1 to 4 carbon atoms, an alkoxybenzoyl group wherein the alkyl group had from 1 to 4 carbons, a halobenzoyl group, or a group ##STR2## where together R.sup.10 and R.sup.11 form a C.sub.3 to C.sub.7 alkylene group, and R.sup.12 and R.sup.13 are each alkyl from 1 to 4 carbon atoms.Type: GrantFiled: October 31, 1988Date of Patent: August 7, 1990Assignee: The University of North Carolina at Chapel HillInventors: Robert A. Izydore, Iris H. Hall
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Patent number: 4943584Abstract: Novel (p-phenoxyphenoxy)-methyl-five-membered heeroaromatic radicals of the formula ##STR1## where the substituents have the following meanings: R.sup.1, R.sup.2, R.sup.3 hydrogen, halogen, C.sub.1 -C.sub.8 -alkyl, C.sub.1 -C.sub.8 -alkoxy, C.sub.1 -C.sub.4 -haloalkyl, C.sub.1 -C.sub.4 -haloalkoxy, C.sub.3 -C.sub.10 -cycloalkyl, nitro or cyano,R.sup.4 hydrogen or C.sub.1 -C.sub.4 -alkyl, and a five-membered heteroaromatic ring, and their use for combating pests.Type: GrantFiled: April 20, 1988Date of Patent: July 24, 1990Assignee: BASF AktiengesellschaftInventors: Hans Theobald, Christoph Kuenast, Peter Hofmeister, Hans-Juergen Neubauer, Thomas Kuekenhoehner, Wolfgang Krieg, Joachim Leyendecker, Uwe Kardorff
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Patent number: 4940575Abstract: 4-Hydroxyisoxazole derivatives corresponding to the formula: ##STR1## wherein: R represents a linear or branched alkyl or hydroxyalkyl radical with 1 to 23 carbon atoms, a linear or branched alkenyl radical with 2 to 23 carbon atoms, a phenyl radical, or a benzyl radical, andR.sub.1 represents OR.sub.2, --NHR.sub.3, or --NH--NHR.sub.4,R.sub.2 represents a hydrogen atom or an alkyl radical with 1 to 24 carbon atoms,R.sub.3 represents a hydrogen atom, an alkyl radical with 1 to 20 carbon atoms, or a ##STR2## radical, where n is 2 to 3 and r' and r" are identical or different, representing a hydrogen atom or a lower alkyl radical or forming a heterocycle when taken together such as morpholine, piperidine, or piperazine,R.sub.4 represents a hydrogen atom or a benzyl radical,and the salts of the formula (I) compounds.These derivatives are applicable to therapeutic and cosmetic fields, in particular to counteract the harmful effects of the sun.Type: GrantFiled: June 26, 1989Date of Patent: July 10, 1990Assignee: Societe Anonyme dite:L'OrealInventors: Alexandre Zysman, Henri Sebag
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Patent number: 4937255Abstract: For inhibiting 3-hydroxy-3-methylglutaryl coenzyme A and cholesterol biosynthesis, the novel disubstituted pyrroles of the formula ##STR1## in which R.sup.1 is aryl or heteroaryl,R.sup.2 is cycloalkyl or optionally substituted alkyl,R.sup.3 is hydrogen or cycloalkyl, or optionally substituted alkyl, aryl or heteroaryl,X is --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH--,A is ##STR2## R.sup.6 is hydrogen or alkyl, and R.sup.7 is hydrogen, a cation or alkyl, aryl or aralkyl.Type: GrantFiled: March 16, 1989Date of Patent: June 26, 1990Assignee: Bayer AktiengesellschaftInventors: Walter Hubsch, Rolf Angerbauer, Peter Fey, Hilmar Bischoff, Dieter Petzinna, Delf Schmidt, Gunter Thomas
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Patent number: 4933464Abstract: A one-step process to form 3-phenylisoxazolines and 3-phenylisoxazoles by contacting a benzyl halide, a nitrite and an olefin or acetylenic compound, respectively, in the presence of a phase transfer agent.Type: GrantFiled: April 25, 1988Date of Patent: June 12, 1990Assignee: W. R. Grace & Co.-Conn.Inventor: Sheldon B. Markofsky
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Patent number: 4929630Abstract: The present invention is directed to certain 3,5 substituted, 4,5-dihydroisoxazoles, and methods for their use. These compounds are transglutaminase inhibitors, and are particularly effective in the inhibition of epidermal transglutaminase and the treatment of acne.Type: GrantFiled: September 8, 1989Date of Patent: May 29, 1990Assignee: Syntex (U.S.A.) Inc.Inventors: Arlindo L. Castelhano, Lawrence M. DeYoung, Alexander Krantz, Diana H. Pliura, Michael C. Venuti
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Patent number: 4924002Abstract: The present invention is a process in which isoxazoles are treated with Mo(CO).sub.6 and then hydrazine to obtain corresponding pyrazoles.Type: GrantFiled: February 13, 1989Date of Patent: May 8, 1990Assignee: Warner-Lambert CompanyInventor: Catherine R. Kostlan
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Patent number: 4914206Abstract: The present invention provides lankacidin derivatives of the formula ##STR1## and procedures for the production thereof. The lankacidin derivatives [1] show excellent antimicrobial activities and thus can be used for prophylaxis and treatment of infectious disease in animals.Type: GrantFiled: December 15, 1988Date of Patent: April 3, 1990Assignee: Takeda Chemical Industries, LTD.Inventors: Isao Minamida, Naoto Hashimoto
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Patent number: 4912120Abstract: The present invention is directed to certain 3,5 substituted, 4,5-dihydroisoxazoles, and methods for their use. These compounds are transgulatminase inhibitors, and are particularly effective in the inhibition of epidermal transglutaminase and the treatment of acne.Type: GrantFiled: March 13, 1987Date of Patent: March 27, 1990Assignee: Syntex (U.S.A.) Inc.Inventors: Arlindo L. Castelhano, Lawrence M. DeYoung, Alexander Krantz, Diana H. Pliura, Michael C. Venuti
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Patent number: 4910313Abstract: The present invention is related to new diselenobis benzoic acid amides of primary heterocyclic amines of the general formula I ##STR1## process for producing the same and process for treating certain diseases in human beings by administration of the same to the humans suffering from such diseases.Type: GrantFiled: August 6, 1987Date of Patent: March 20, 1990Assignee: Nattermann & CIE GmbHInventors: Andre Welter, Axel Roemer, Sigurd Leyck, Michael J. Parnham
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Patent number: 4904660Abstract: Novel compounds of the following formula (I) and their salts: A compound of the formula (I) ##STR1## These compounds are expected to be useful for renin inhibitors. Thus, the compounds are useful medical agents, in particular, anti-hypertensive agents.Type: GrantFiled: February 25, 1988Date of Patent: February 27, 1990Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Kohji Nakano, Takashi Fujikura, Ryuichiro Hara, Masato Ichihara, Yukiko Fukunaga, Masayuki Shibasaki
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Patent number: 4897489Abstract: The compounds of the formula: ##STR1## wherein R.sup.1 is hydrogen, amino, isonitrile or an organic residue bonded through nitrogen; R.sup.2 is carboxy or a group derivable therefrom; X is hydrogen, methoxy, formylamino, alkyl which may be substituted, alkylthio in which the sulfur atom may be oxidized or azido, or forms a double bond together with the adjacent carbon atom; provided that when R.sup.1 is acetylamino or amino and X is hydrogen, R.sup.2 is not para-nitrobenzyloxycarbonyl or benzhydryloxycarbonyl, or a pharmaceutically acceptable salt thereof, exhibit excellent antimicrobial activity, and are utilized as antimicrobial agents.Type: GrantFiled: May 21, 1987Date of Patent: January 30, 1990Assignee: Takeda Chemical Industries, Ltd.Inventors: Kouichi Yoshioka, Setsuo Harada, Michihiko Ochiai, Hirotomo Masuya
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Patent number: 4895864Abstract: As the novel antibiotic TAN-950A having the structural formula ##STR1## and salt thereof of the present invention show antimicrobial action against fungi, they can be used in the therapeutics of fungal infections, in human and other animals etc. by oral, parenteral or external administration.Type: GrantFiled: April 22, 1988Date of Patent: January 23, 1990Assignee: Takeda Chemical Industries, Ltd.Inventors: Takashi Iwasa, Shigetoshi Tsubotani, Setsuo Harada
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Patent number: 4892870Abstract: A novel class of 5, 6 or 7 member heterocycles which belong to the 3-isoxazolidinone, 2H-1,2-oxazin-3 (4H)-one and 3-isoxazepinone series of compounds and which are substituted at the 4-carbon by a benzylidene radical. The compounds have utility as analgesic agents, immunomodulating agents, anti-inflammatory agents and anti-pyretic agents and they may be combined with excipients to provide formuations which are useful in treating arthritis and conditions generally associated with that disease.Type: GrantFiled: August 1, 1988Date of Patent: January 9, 1990Assignee: Biofor, Ltd.Inventor: Sung J. Lee
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Patent number: 4892578Abstract: Novel 2-[(4-substituted phenyl)methyl]-4,4-dimethyl-3-isoxazolidinone plant regulators of the following structural formula ##STR1## or an agriculturally acceptable salt thereof, agricultural compositions thereof and a method for regulation growth and development of plant growth therewith are disclosed and exemplified.Type: GrantFiled: November 6, 1987Date of Patent: January 9, 1990Assignee: FMC CorporationInventors: Jun H. Chang, Jonathan S. Baum
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Patent number: 4892882Abstract: Compounds of formula (I): ##STR1## (wherein: R.sup.1 represents a hydrogen atom or a halogen atom;R.sup.2 represents a C.sub.1 -C.sub.6 alkyl group; andA represents an oxygen atom, a sulphur atom, a sulphinyl group or a sulphonyl group)have good insecticidal activity coupled with a low toxicity to warm-blooded animals. Compounds in which A represents an oxygen or sulphur atom can be prepared by reacting a corresponding alkali metal alkoxide or mercaptide with the corresponding 3-dimethylcarbamoyloxy-5-halomethylisoxazole derivative, while compounds where A represents a sulphinyl or sulphonyl group may be prepared by oxidizing the corresponding compound wherein A represents a sulphur atom. The compounds may be formulated with conventional insecticidal carriers or diluents and exhibit a synergistic increase in activity when combined with various known organic phosphate and carbamate insecticides.Type: GrantFiled: January 18, 1985Date of Patent: January 9, 1990Assignee: Sankyo Company LimitedInventors: Kazuo Tomita, Tadashi Murakami, Hideakira Tsuji, Keigo Matsumoto, Katsuhiro Fujita