Spiro Patents (Class 548/407)
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Patent number: 5171742Abstract: Avermectin analogs are disclosed wherein the 6,6-spiroketal ring system has been reduced in size to a 6,5-spiroketal ring system by the deletion of the 25-position carbon atom and the 25-alkyl substituent and which has a 23-acyl cycloalkyl, phenyl or substituted hydroxymethyl substituent. This is accomplished by opening the outer spiroketal ring with the elimination of ring carbon atoms 23, 24 and 25 and the alkyl substituent at the 25-position and incorporation a new component, reclosing the spiroketal to a 5-membered ring with a 23-acyl substituent and new substituents at the 24-position. The compounds are used as anti-parasitic insecticidal and anti-helmintic agents in humans and animals and compositions containing such compounds as the active ingredient thereof are also disclosed.Type: GrantFiled: October 15, 1991Date of Patent: December 15, 1992Assignee: Merck & Co., Inc.Inventor: Peter T. Meinke
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Patent number: 5166350Abstract: A process for the preparation of a fluoran compound of the formula ##STR1## wherein R, R.sub.1, R.sub.2 and R.sub.4 are each independently hydrogen, halogen, lower alkyl or lower alkoxy,R.sub.3 is hydrogen, halogen, lower alkyl, lower alkoxy or --NX.sub.3 X.sub.4, or (R.sub.1 and R.sub.2) or (R.sub.3 and R.sub.4) each pair together with the carbon atoms to which they are attached, form a fused benzene nucleus,X.sub.1, X.sub.2, X.sub.3 and X.sub.4 are each independently hydrogen, alkyl containing not more than 12 carbon atoms which is unsubstituted or substituted by cyano, halogen, hydroxy, tetrahydrofuryl or lower alkoxy, or are cycloalkyl, aryl or aralkyl or (X.sub.1 and X.sub.2) or (X.sub.3 and X.sub.Type: GrantFiled: September 30, 1991Date of Patent: November 24, 1992Assignee: Ciba-Geigy CorporationInventors: Davor Bedekovic, Jerry L. Pool, Brian J. Williams, Robert Garner, John B. Henshall
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Patent number: 5162550Abstract: Bisphthalide lactones of formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are each independently of one another hydrogen, alkyl of at most 12 carbon atoms which is unsubstituted or substituted by halogen, hydroxy, cyano, tetrahydrofuryl or lower alkoxy; or are acyl of 1 to 12 carbon atoms, cycloalkyl of 5 to 10 carbon atoms or unsubstituted aralkyl or aryl, or aralkyl or aryl each substituted by halogen, cyano, nitro, trifluormethyl, lower alkyl, lower alkoxy, lower alkoxycarbonyl, --NX'X"-- or 4--NX'X--"phenylamino, wherein X' and X" are each independently of the other hydrogen, lower alkyl, cyclohexyl, benzyl or phenyl, or the pairs of substituents --NR.sub.1 R.sub.2 and --NR.sub.3 R.sub.4 are each a 5- or 6-membered, preferably saturated, heterocyclic radical, V.sub.1 and V.sub.2 are hydrogen, halogen, lower alkyl, C.sub.1 -C.sub.12 alkoxy, C.sub.1 -C.sub.Type: GrantFiled: August 24, 1990Date of Patent: November 10, 1992Assignee: Ciba-Geigy CorporationInventors: Rudolf Zink, Ian J. Fletcher
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Patent number: 5130058Abstract: A photochromic compound represented by the following general formula [I] ##STR1## wherein ##STR2## represents a divalent aromatic hydrocarbon group or a divalent heterocyclic group each of which may have a substituent,R.sub.1 represents a monovalent hydrocarbon group or a monovalent heterocyclic group each of which may have a substituent, ##STR3## represents a norbornylidene or adamantylidene group which may have a substituent,X represents an oxygen atom or a group of the formula >N--R.sub.3 in which R.sub.3 represents a hydrogen atom or a hydrocarbon group which may have a substituent, andR.sub.2 represents a monovalent hydrocarbon group which may have a substituent.Also provided are a process for production of the photochromic compound, a composition containing the photochromic compound, and the use of the photochromic compound. The colored form of this photochromic compound has excellent thermal stability.Type: GrantFiled: June 29, 1989Date of Patent: July 14, 1992Assignee: Tokuyama Soda Kabushiki KaishaInventors: Takashi Tanaka, Kenji Tanaka, Satoshi Imura, Yasuji Kida
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Patent number: 5126460Abstract: A process for the preparation of a pure (3S,4R)-isomer of a compound of formula (A): ##STR1## wherein the substituents are herein defined in which the pyrrolidonyl or piperidonyl ring is formed by cyclizing an appropriate precursor dihydrobenzopyranol compound that has already been resolved to the (3S,4R)-configuration, or a mixture in which the (3S,4R)-configuration predominates with respect to the (3S,4R)-configuration.Type: GrantFiled: January 30, 1990Date of Patent: June 30, 1992Assignee: Beecham Group p.l.c.Inventor: Erol A. Faruk
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Patent number: 5118702Abstract: Fungicidal and microbicidal substituted 1-aminomethyl-3-aryl-4-cyano-pyrroles of the formula ##STR1## in which Ar represents optionally substituted phenyl,R.sup.1 represents optionally substituted alkyl, alkenyl, alkynyl or cycloalkyl or in each case optionally substituted aralkyl or aryl andR.sup.2 represents alkyl or in each case optionally substituted cycloalkylalkyl, aralkyl, cycloalkyl or aryl,and their acid addition salts.Type: GrantFiled: December 17, 1990Date of Patent: June 2, 1992Assignee: Bayer AktiengesellschaftInventors: Detlef Wollweber, Wolfgang Kramer, Wilhelm Brandes, Stefan Dutzmann, Wilfried Paulus
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Patent number: 5116968Abstract: Compounds of formula (1) ##STR1## wherein R represents a sugar residue or an acylated derivative thereof;R.sup.1 represents a methyl, ethyl or isopropyl group;Y.sup.1 is --CH.sub.2, Y.sup.2 is --CH-- and X represents ##STR2## [wherein R.sup.2 represents a hydrogen atom or a group OR.sup.6 (where OR.sup.6 is a hydroxyl group or a substituted hydroxyl group having up to 25 carbon atoms) and R.sup.3 represents a hydrogen atom, or R.sup.2 and R.sup.3 together with the carbon atom to which they are attached represent >C.dbd.0, >C.dbd.CH.sub.2 or >C.dbd.NOR.sup.7 (where R.sup.7 represents a hydrogen atom, a C.sub.1-8 alkyl group or a C.sub.3-8 alkenyl group) and the group >C.dbd.NOR.sup.7 is in the E configuration] or --Y.sup.1 --X--Y.sup.2 -- represents --CH.dbd.CH--CH-- or --CH.sub.2 --CH.dbd.C--; andR.sup.4 represents a group OR.sup.6 as defined above and R.sup.5 represents a hydrogen atom, or R.sup.4 and R.sup.5 together with the carbon atom to which the are attached represent >C.dbd.0 or >C.Type: GrantFiled: December 20, 1990Date of Patent: May 26, 1992Assignee: American Cyanamid CompanyInventors: Gordon C. Lawrence, Michael J. Dawson, David Noble, Michael V. J. Ramsay, Richard Bell, Derek R. Sutherland, Edward P. Tiley
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Patent number: 5108992Abstract: Compounds of formula (1) ##STR1## and their salts, wherein R.sup.1 is a methyl, ethyl or isopropyl group each substituted by a hydroxyl group or R.sup.1 is a group --(CH.sub.2).sub.n R7 or a group --CH(CH.sub.3)R.sup.7 (where n is zero or 1 and R.sup.7 l is CHO or CO.sub.2 H);Y.sup.1 is --CH.sub.2 --, Y.sup.2 is --CH-- and X represents ##STR2## [where R.sup.2 is a hydrogen atom or a group OR.sup.8 is a hydroxyl group or a substituted hydroxyl group having up to 25 carbon atoms) and R.sup.3 is a hydrogen atom, or R.sup.2 and R.sup.3 together with the carbon atom to which they are attached represent >.dbd.O, >C.dbd.CH.sub.2 or >C.dbd.NOR.sup.9 (where R.sup.9 is a hydrogen atom or a C.sub.1-8 alkyl or C.sub.3-8 alkenyl group) and the group >C.dbd.NOR.sup.9 is in the E configuration] or --Y.sup.1 --X--Y.sup.2 -- represents --CH.dbd.CH--CH-- or --CH.sub.2 --CH.dbd.C--;R.sup.4 is a group OR.sup.8 as defined above and R.sup.5 is a hydrogen atom, or R.sup.4 and R.sup.Type: GrantFiled: December 20, 1990Date of Patent: April 28, 1992Assignee: American Cyanamid CompanyInventors: Gordon C. Lawrence, Michael J. Dawson, David Noble, Richard A. Fletton, Stephen J. Lane
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Patent number: 5097045Abstract: An improved process for the preparation of trans-6-[2-(substituted-pyrrol-1-yl)alkyl]pyran-2-ones by a novel synthesis is described where 1,6-heptadien-4-ol is converted in eight operations to the desired products, as well as an improved process for the preparation of (2R-trans) and trans-(.+-.)-5-(4-fluorophenyl)-2-(1-methylethyl)-N,4-diphenyl-1-[2-(tetra hydro-4-hydroxy-6-oxo-2H-pyran-2-yl)ethyl]1H-pyrrole-3-carboxamide by a novel synthesis where 4-methyl-3-oxo-N-phenylpentanamide is converted in eight operations to the desired product or alternatively 4-fluoro-.alpha.-[2-methyl-1-oxopropyl]-.gamma.-oxo-N,.beta.-diphenylbenze nebutaneamide is converted in one step to the desired product, and additionally, a process for preparing (2R-trans)-5-(4-fluorophenyl)-2-(1-methylethyl)-N,4-diphenyl-1-[2-(tetrahy dro-4-hydroxy-6-oxo-2H-pyran-2-yl)ethyl]-1H-pyrrole-3-carboxamide from (R)-4-cyano-3-[[(1,1-dimethylethyl)dimethylsilyl]oxy]butanoic acid, as well as other valuable intermediates used in the processes.Type: GrantFiled: October 9, 1990Date of Patent: March 17, 1992Assignee: Warner-Lambert CompanyInventors: Donald E. Butler, Carl F. Deering, Alan Millar, Thomas N. Nanninga, Bruce D. Roth
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Patent number: 5068245Abstract: N-Substituted 3-arylpyrrolidine derivatives of the formula ##STR1## where R.sup.1 is 2,2-dimethylpropyl, 3,3-dimethylbutyl, 4,4-dimethylpentyl, 2,4,4-trimethylpentyl, 6-methylhept-2-yl, 3,5,5-trimethylhexyl, 6,10-dimethylundec-2-yl, 3-methylcyclohexyl, 3,3-dimethylcyclohexyl, 3,3,5-trimethylcyclohexyl, 3,3,5,5-tetramethylcyclohexyl, 4-methylcyclohexyl, 4-ethylcyclohexyl, 4-propylcyclohexyl, 4-isopropylcyclohexyl, 4-tert.-butylcyclohexyl, trans-4-tert.-butylcyclohexyl, 4(2-methylbut-2-yl)cyclohexyl, 4(2,4,4-trimethylpent-2-yl)-cyclohexyl, cyclododecanyl, C.sub.3 -C.sub.9 -trialkylsilyl-substituted C.sub.4 -C.sub.12 -cycloalkyl, 4-hydroxycyclohexyl, 4-hydroxy-3-methylcyclohexyl, 4-hydroxy-3,5-dimethylcyclohexyl, 4-hydroxy-3,3-dimethylcyclohexyl, 4-hydroxy-3,3,5-trimethylcyclohexyl, unsubstituted or hydroxy-, C.sub.1 -C.sub.9 -alkyl-, C.sub.1 -C.sub.5 -alkoxy- or C.sub.3 -C.sub.9 -trialkylsilyl-substituted C.sub.5 -C.sub.12 -cycloalkenyl,R.sup.1 is further bicycloalkyl,R.sup.1 is further 4-tert.Type: GrantFiled: September 30, 1988Date of Patent: November 26, 1991Assignee: BASF AktiengesellschaftInventors: Matthias Zipplies, Hubert Sauter, Franz Roehl, Walter Himmele, Eberhard Ammermann, Ernst-Heinrich Pommer
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Patent number: 5068246Abstract: 3-Alkyl-4-arylpyrrolidine derivatives of the formula ##STR1## where R.sup.1 is alkenyl, alkynyl, cycloalkyl, cycloalkenyl, alkyl-cycloalkyl, cycloalkyl-alkyl, alkyl-cycloalkyl-alkyl, cycloalkenyl-alkyl, alkyl-cycloalkenyl, bicycloalkyl, bicycloalkylalkyl, alkyl-bicycloalkyl, heterocycloalkyl, heterocycloalkylmethyl, aryl, arylalkyl, alkylary, alkyl-aryl-alkyl,R.sup.2 is alkyl, alkoxy,R.sup.3 is alkylR.sup.4 is alkyl, alkenyl, alkynyl and phenylalkyl,X.sup.- is a plant-tolerated anion, andn is 0 or 1,their plant-tolerated salts, and fungicides containing these compounds.Type: GrantFiled: September 30, 1988Date of Patent: November 26, 1991Assignee: BASF AktiengesellschaftInventors: Matthias Zipplies, Hubert Sauter, Walter Himmele, Eberhard Ammermann, Ernst-Heinrich Pommer
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Patent number: 5066814Abstract: 2-Dicarboximidefluorane or 3-dicarboximidefluorane compounds of the formula ##STR1## in which R.sub.1 and R.sub.2 independently of one another are each hydrogen, halogen, lower alkyl or lower alkoxy, one of Z.sub.1 and Z.sub.2 is the dicarboximide group ##STR2## and the other is hydrogen, halogen, lower alkyl or lower alkoxy, W is a radical of a dicarboxylic acid containing at least 2 carbon atoms, X.sub.1 and X.sub.2 are hydrogen, alkyl which is unsubstituted or substituted by halogen, hydroxyl, cyano, tetrahydrofuryl or lower alkoxy, cycloalkyl, or benzyl or phenyl each of which is unsubstituted or substituted by halogen, cyano, nitro, lower alkyl, lower alkoxy, lower alkoxycarbonyl, --NX'X" or -4-NX'X"-phenylamino in which X' and X" independently of one another are hydrogen, lower alkyl, cyclohexyl, benzyl or phenyl, or X.sub.1 and X.sub.Type: GrantFiled: February 23, 1990Date of Patent: November 19, 1991Assignee: Ciba-Geigy CorporationInventor: Rudolf Zink
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Patent number: 5066490Abstract: Crosslinking reagents for amino group-containing compounds are provided, which crosslinkers can be cleaved under mildly acidic conditions. The crosslinkers can be used to crosslink biologically active substances to be delivered to the cells, wherein the crosslinker will be cleaved in the mildly acidic conditions within the cell.Type: GrantFiled: June 1, 1988Date of Patent: November 19, 1991Assignee: The United States of America as represented by the Secretary of the Department of Health & Human ServicesInventors: David M. Neville, Jr., Kasturi Srinivasachar
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Patent number: 5061813Abstract: Novel compounds are disclosed having the formula ##STR1## and R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6 and R.sub.7 are as defined herein. These compounds are useful, for example, as cardiovascular agents and especially as anti-ischemic agents.Type: GrantFiled: April 2, 1990Date of Patent: October 29, 1991Assignee: E. R. Squibb & Sons, Inc.Inventor: Karnail Atwal
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Patent number: 5043347Abstract: A compound selected from the group consisting of enantiomers and diastereoisomer forms and mixtures thereof of the formula ##STR1##Type: GrantFiled: November 17, 1989Date of Patent: August 27, 1991Assignee: Roussel UclafInventors: Francois Clemence, Odile Le Martret, Francoise Delevallee, Michel Fortin
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Patent number: 5028711Abstract: Benzopyran derivatives of the general formula I ##STR1## are disclosed. The compounds are therapeutic active compounds.Type: GrantFiled: July 6, 1989Date of Patent: July 2, 1991Assignee: Beiersdorf AktiengesellschaftInventors: Wolfgang Stenzel, Theo Schotten, Ben Armah
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Patent number: 5021423Abstract: Mitomycin derivatives having the formula ##STR1## wherein X is acyl, lower alkyl, alkoxycarbonyl aryloxycarbonyl or aralkoxycarbonyl;Y is hydrogen or methyl;Z is hydrogen, methyl, acyl or allyloxycarbonyl;one of R.sub.1 and R.sub.2 represents carbamoyloxymethyl and the other represents hydrogen, or R.sub.1 and R.sub.2 together represent methylene, show antibacterial and antitumor activities.Type: GrantFiled: May 26, 1989Date of Patent: June 4, 1991Assignee: Kyowa Hakko Kogyo Kabushiki KaishaInventors: Yutaka Kanda, Hitoshi Arai, Masaji Kasai, Makoto Morimoto
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Patent number: 5019588Abstract: Novel 1,2-cyclohexylaminoaryl amides useful as analgesic agents having very high kappa-opioid affinity and selectivity and potency and useful as analgesics, diuretics, antiinflammatory and psychotherapeutic agents are disclosed. Methods for making the compounds and pharmaceutical compositions containing them are also disclosed.Type: GrantFiled: October 10, 1989Date of Patent: May 28, 1991Assignee: Warner-Lambert CompanyInventors: David C. Horwell, David C. Rees
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Patent number: 5013827Abstract: Triggerable dioxetanes with a fluorescent molecule containing group bonded or tethered in the dioxetane so as to produce fluorescence from the group are described. The compounds are useful in immunoassays and in probes using enzymes or other chemicals for triggering the dioxetanes to produce light from the fluorescent molecule in the group as a signal.Type: GrantFiled: November 13, 1989Date of Patent: May 7, 1991Assignee: Board of Governors of Wayne State UniversityInventor: Arthur P. Schaap
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Patent number: 5001145Abstract: Compounds are described of formula (1) ##STR1## and salts thereof wherein R.sup.1 is a methyl, ethyl or isopropyl group;R.sup.2 represents a hydrogen atom or a group OR.sup.4 (where OR.sup.4 is a hydroxyl group or a substituted hydroxyl group having up to 25 carbon atoms) and R.sup.3 represents a hydrogen atom, or R.sup.2 and R.sup.3 together with the carbon atom to which they are attached represent >C.dbd.CH.sub.2, >C.dbd.O or >C.dbd.NOR.sup.5 (where R.sup.5 is a hydrogen atom or a C.sub.1-8 alkyl group and the group >C.dbd.NOR.sup.5 is in the E configuration).These compounds may be used for controlling insect, acarine, nematode or other pests.Type: GrantFiled: January 27, 1989Date of Patent: March 19, 1991Assignee: American Cyanamid CompanyInventors: Michael V. J. Ramsay, Derek N. Evans, Derek R. Sutherland, Edward P. Tiley, John B. Ward, Neil Porter, Hazel M. Noble, Richard A. Fletton, David Noble
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Patent number: 5001128Abstract: Disclosed are novel 3-hydroxy-3-methylglutarylcoenzyme A reductase inhibitors useful as antihypercholesterolemic agents represented by the formula ##STR1## and the corresponding ring-opened hydroxy acids and esters derived therefrom and pharmaceutically acceptable salts thereof.Pharmaceutical compositions containing said compounds and method of inhibiting the biosynthesis of cholesterol therewith are also disclosed.Type: GrantFiled: December 15, 1989Date of Patent: March 19, 1991Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.Inventors: Kent W. Neuenschwander, Anthony C. Scotese
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Patent number: 4987138Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein: either one of R.sub.1 and R.sub.2 is hydrogen and the other is selected from the class of C.sub.1-6 alkylcarbonyl, C.sub.1-6 alkoxycarbonyl, C.sub.1-6 alkylcarbonyloxy, C.sub.1-6 alkylhydroxymethyl, nitro, cyano, chloro, trifluoromethyl, C.sub.1-6 alkylsulphinyl, C.sub.1-6 alkylsulphonyl, C.sub.1-6 alkoxysulphinyl, C.sub.1-6 alkoxysulphonyl, C.sub.1-6 alkylcarbonylamino, C.sub.1-6 alkoxycarbonylamino, C.sub.1-6 alkyl-thiocarbonyl, C.sub.1-6 alkoxy-thiocarbonyl, C.sub.1-6 alkyl-thiocarbonyloxy, 1-mercapto C.sub.2-7 alkyl, formyl or aminosulphinyl, aminosulphonyl or aminocarbonyl, the amino moiety being optionally substituted by one or two C.sub.1-6 alkyl groups, or C.sub.1-6 alkylsulphinylamino, C.sub.1-6 alkylsulphonylamino C.sub.1-6 alkoxysulphinylamino or C.sub.1-6 alkoxysulphonylamino or ethenyl terminally substituted by C.sub.1-6 alkylcarbonyl, nitro or cyano, or --C(C.sub.1-6 alkyl(NOH) or --C(C.sub.1-6 alkyl)NNH.Type: GrantFiled: August 11, 1988Date of Patent: January 22, 1991Assignee: Beecham Group p.l.c.Inventors: Frederick Cassidy, Geoffrey Stemp
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Patent number: 4985421Abstract: Fungicidal substituted dioxolanylethylamine of the formula ##STR1## in which R represents alkyl, or represents in each case optionally substituted cycloalkylalkyl, aralkyl, cycloalkyl or aryl, andR.sup.1 and R.sup.2 independently of one another each represents hydrogen, alkyl, alkenyl, alkinyl, alkoxyalkyl, dialkoxyalkyl, hydroxyalkyl, hydroxyalkoxyalkyl, alkoxycarbonylalkyl, dioxolanylalkyl, dioxanylalkyl or oxolanylalkyl, or represents in each case optionally substituted cycloalkylalkyl, cycloalkyl, aralkyl, aralkenyl or aryl, orR.sup.1 and R.sup.2, together with the nitrogen atom to which they are bonded, represent an optionally substituted saturated heterocyclic radical, which can optionally contain further hetero atoms,and acid addition salts thereof.Intermediates wherein the amino group is an electron-withdrawing leaving group are also new.Type: GrantFiled: August 17, 1989Date of Patent: January 15, 1991Assignee: Bayer AktiengesellschaftInventors: Wolfgang Kramer, Joachim Weissmuller, Dieter Berg, Wilhelm Brandes, Stefan Dutzmann
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Patent number: 4981976Abstract: Cyanatoaryl-substituted 1,6-diaza[4.4]spirodilactam having a cyanatoaryl-containing substituent on each spiro ring nitrogen atom self-cure upon application of heat to produce cured, crosslinked thermoset resins of high glass transition temperature.Type: GrantFiled: February 23, 1989Date of Patent: January 1, 1991Assignee: Shell Oil CompanyInventor: Pen C. Wang
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Patent number: 4973712Abstract: Novel 2-aralkylaminofluorans of formula ##STR1## wherein Q is --CH.sub.2 --, --CH.sub.2 --O-- or --CO--,R.sub.1, R.sub.2 and R.sub.3 are each independently of one another hydrogen, halogen, lower alkyl or lower alkoxy,X.sub.1 and X.sub.2 are each independently of the other hydrogen, alkyl which is unsubstituted or substituted by halogen, hydroxy, cyano, tetrahydrofuryl or lower alkoxy, or ar cycloalkyl or benzyl or phenyl, each unsubstituted or substituted by halogen, cyano, nitro, lower alkyl, lower alkoxy or lower alkoxycarbonyl; or--NX.sub.1 X.sub.2 is a 5- 6-membered heterocyclic radical, and wherein the benzene rings A and B are independently of the other unsubstituted or substituted by halogen, cyano, lower alkyl, lower alkoxy, lower alkylthio, lower alkoxycarbonyl or trifluoromethyl, and the ring D is unsubstituted or substituted by halogen, nitro, lower alkyl, lower alkoxy, lower alkylthio, amino, mono-lower alkylamino or di-lower alkylamino.Type: GrantFiled: February 21, 1989Date of Patent: November 27, 1990Assignee: Ciba-Geigy CorporationInventor: Rudolf Zink
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Patent number: 4970309Abstract: This invention relates to a novel method of synthesizing di- and triarylmethane dye precursor compounds possessing a thiolactone ring-closing moiety, from the corresponding lactones.Type: GrantFiled: December 7, 1989Date of Patent: November 13, 1990Assignee: Polaroid CorporationInventor: Patrick F. King
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Patent number: 4963568Abstract: Novel compounds which are selective dopamine agonists are useful for treating disorders characterized by abnormal dopamine levels, such as Parkinson's Disease, as well as cardiovascular disorders.Type: GrantFiled: May 31, 1989Date of Patent: October 16, 1990Assignee: Abbott LaboratoriesInventors: Robert W. Schoenleber, John W. Kebabian, Yvonne C. Martin, Michael P. DeNinno, Richard J. Perner, David M. Stout, Chi-Nung W. Hsiao, Stanley DiDomenico, Jr., John F. DeBernardis, Fatima Z. Basha, Michael D. Meyer, Biswanath De
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Patent number: 4963538Abstract: Novel HMG-CoA reductase inhibitors are useful as antihypercholesterolemic agents and are represented by structural formulae (I) or (II): ##STR1## wherein position 5 of the polyhydronaphthyl ring is singly or doubly bonded to oxygen or incorporated into a C.sub.3-7 carbocyclic ring.Type: GrantFiled: March 13, 1989Date of Patent: October 16, 1990Assignee: Merck & Co., Inc.Inventors: Mark E. Duggan, George D. Hartman
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Patent number: 4954631Abstract: Fluoran compounds are disclosed of formula (I) ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 independently represent hydrogen, halogen, lower alkoxy, C.sub.1 -C.sub.9 -alkyl, C.sub.5 or C.sub.6 -cycloalkyl, benzyl or phenyl, said benzyl or phenyl being optionally substituted by halogen, lower alkyl or lower alkoxy, and further R.sub.1 and R.sub.2 as well as R.sub.3 and R.sub.4 taken together with Ring A, may form a naphthalene ring optionally substituted by halogen, lower alkyl or lower alkoxy, R.sub.5, R.sub.6 and R.sub.7 independently represent halogen, lower alkyl or lower alkoxy, B.sub.1 and B.sub.2 independently represent hydrogen, C.sub.1 -C.sub.8 -alkyl, benzyl or phenyl, said benzyl or phenyl being optionally substituted by halogen, lower alkyl, lower alkoxy, or alkyl-substituted, X represents hydrogen atom or --NR.sub.8 R.sub.9 wherein R.sub.8 and R.sub.9 independently represent hydrogen, C.sub.1 -C.sub.8 -alkyl, C.sub.5 or C.sub.Type: GrantFiled: February 2, 1989Date of Patent: September 4, 1990Assignee: Shin Nisso Kako Co., Ltd.Inventors: Takeo Obitsu, Yutaka Ohnishi, Shinji Yoshinaka, Minoru Koguchi, Mitsuhiro Yanagita, Nobuyuki Hirai
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Patent number: 4943582Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein: X, Y and R.sub.1 -R.sub.6 are as defined have blood pressure lowering activity and K+ channel activator activity and are useful in the treatment of hypertension.Type: GrantFiled: May 1, 1987Date of Patent: July 24, 1990Assignee: Beecham Group p.l.c.Inventors: John M. Evans, Geoffrey Stemp, Frederick Cassidy
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Patent number: 4882438Abstract: A compound represented by the following general formula [I] ##STR1## wherein ##STR2## represents a norbornylidene group or an adamantylidene group each of which may have a substituent, andX represents an oxygen atom, the group >N-R.sub.2, the group >N-A.sub.1 -B.sub.1 --A.sub.2).sub.m (B.sub.2).sub.n R.sub.3, the group >N-A.sub.3 -A.sub.4, or the group >N-A.sub.3 -R.sub.4, provided that when ##STR3## is an adamantylidene group, X is selected from the above groups excepting the oxygen atom and the group >N-R.sub.2 ; and plastic lens containing the compound of the above formula [I].Type: GrantFiled: November 8, 1988Date of Patent: November 21, 1989Assignee: Tokuyama Soda Kabushiki KaishaInventors: Takashi Tanaka, Satoshi Imura, Yasuji Kida
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Patent number: 4880825Abstract: Mitomycin derivatives having potent anti-tumor activity having the formula: ##STR1## wherein one of R.sub.1 and R.sub.2 represents carbamoyloxymethyl and the other represents hydrogen or R.sub.1 and R.sub.2 are bonded together to form methylene;X is hydrogen or halogen;Y is hydrogen or methyl;Z is hydrogen, methyl or acyl; andn is an integer of 2 or 3.Type: GrantFiled: March 25, 1988Date of Patent: November 14, 1989Assignee: Kyowa Hakko Kogyo Kabushiki KaishaInventors: Masaji Kasai, Yutaka Kanda, Motomichi Kono, Yutaka Saito, Makoto Morimoto, Tadashi Ashizawa
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Patent number: 4876359Abstract: Novel .gamma.-butyrolactone derivatives having strong ACE inhibitory activity are provided. They are represented by the following general formula (I): ##STR1## wherein R.sup.1 and R.sup.2 may be the same or different and mean individually a hydrogen atom or a straight-chain or branched alkyl or cycloalkyl group, or R.sup.1 and R.sup.2 are bonded together to mean an alkylene group having 2-6 carbon atoms, R.sup.3 denotes a hydrogen atom or a lower alkyl, aralkyl, amino lower alkyl or lower alkoxycarbonylamino lower alkyl group, R.sup.4 means a lower alkyl, cycloalkyl or aralkyl group, R.sup.5 means a hydrogen atom or a lower alkyl group, or R.sub.4 and R.sub.5 are bonded together to denote an alkylene group having 2-4 carbon atoms, and R.sup.6 stands for a hydrogen atom or a lower alkyl or aralkyl group; or a pharmacologically acceptable salt thereof.Type: GrantFiled: October 1, 1987Date of Patent: October 24, 1989Assignee: SS Pharmaceutical Co., Ltd.Inventors: Hiroshi Hasegawa, Noriaki Shioiri, Tadashi Narita, Tatsuhiko Katori
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Patent number: 4871719Abstract: Novel 13-spiro-2'-[tetrahydrofuran]-milbemycins of the formula I ##STR1## in which X represents one of the groups --CH(OR.sub.1)--, --C(.dbd.O)-- or --C(.dbd.N--OH)--;R.sub.1 represents hydrogen or a OH-protecting group;R.sub.2 represents methyl, ethyl, isopropyl or sec.-butyl or the group --C(CH.sub.3).dbd.CH--A in which A represents methyl, ethyl or isopropyl; andR.sub.3 represents hydrogen; C.sub.1 -C.sub.10 -alkyl; C.sub.1 -C.sub.10 -alkyl substituted by at least one substituent selected from the group consisting of halogen, C.sub.1 -C.sub.6 -alkoxy, C.sub.2 -C.sub.6 -alkoxyalkoxy C.sub.3 -C.sub.9 -alkoxyalkoxyalkoxy, C.sub.1 -C.sub.6 -alkylthio, C.sub.3 -C.sub.7 -cycloalkyl, C.sub.1 -C.sub.3 -alkyl-substituted C.sub.3 -C.sub.7 -cycloalkyl, hydroxy, benzyloxy, C.sub.1 -C.sub.6 -acyl and C.sub.1 -C.sub.6 -acyloxy, it being possible for each of the above-mentioned radicals representing or containing an alkoxy group to be terminally substituted at a terminal alkoxy group by hydroxy, halogen, C.sub.1 -C.sub.Type: GrantFiled: March 16, 1988Date of Patent: October 3, 1989Assignee: Ciba-Geigy CorporationInventor: Peter Maienfisch
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Patent number: 4863922Abstract: Aromatic sulfonamides with a saturated heterocycle fused thereto are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure.Type: GrantFiled: June 15, 1988Date of Patent: September 5, 1989Assignee: Merck & Co., Inc.Inventors: John J. Baldwin, Gerald S. Ponticello, Marcia E. Christy
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Patent number: 4851405Abstract: Fungicidally effective aminomethyl heterocyclic compounds of the formula ##STR1## in which X represents oxygen or sulphur,R represents hydrogen or alkyl, or represents in each case optionally substituted cyclohexyl or phenyl andR.sup.1 and R.sup.2 independently of one another each represent hydrogen, alkyl, alkenyl, alkinyl, alkoxyalkyl, dialkoxyalkyl, hydroalkyl, hydroxyalkoxyalkyl, alkoxycarbonylalkyl, dioxolanylalkyl, dioxanylalkyl or oxolanylalkyl, or represent in each case optionally substituted cycloalkylalkyl, cycloalkyl, aralkyl, aralkenyl or aryl, orR.sup.1 and R.sup.2, together with the nitrogen atom to which they are bonded, represent an optionally substituted saturated heterocyclic radical, which can optionally contain further hetero atoms,or acid addition salts thereof.Type: GrantFiled: February 29, 1988Date of Patent: July 25, 1989Assignee: Bayer AktiengesellschaftInventors: Wolfgang Kramer, Joachim Weissmuller, Dieter Berg, Stefan Dutzmann
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Patent number: 4847376Abstract: The present invention provides a lipase substrate of the general formula: ##STR1## wherein A is an alkylene or alkenylene radical containing up to 16 carbon atoms, R and R.sub.1, which can be the same or different, each signify an alkyl, alkenyl or acyl radical containing up to 20 carbon atoms or an optionally alkyl-substituted aryl or aralkyl radical containing up to 8 carbon atoms in the alkyl moiety and wherein one of R and R.sub.1 can also be a hydrogen atom, X is the residue of an aromatic hydroxy or thiol compound, and each Y and Z, independently from each other, is --S-- or --O--, Z also --CH.sub.2 --.The present invention also provides a process and a reagent for the optical determination of lipase.Type: GrantFiled: May 1, 1986Date of Patent: July 11, 1989Assignee: Boehringer Mannheim GmbHInventors: Ulrich Neumann, Martina Junius, Hans-Georg Batz
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Patent number: 4831050Abstract: Compounds of formula (I): ##STR1## wherein: either one of R.sub.1 and R.sub.2 is hydrogen and the other is selected from the class of C.sub.1-6 alkylcarbonyl, C.sub.1-6 alkoxycarbonyl, C.sub.1-6 alkylcarbonyloxy, C.sub.1-6 alkylhydroxymethyl, nitro, cyano, chloro, trifluoromethyl, C.sub.1-6 alkylsulphinyl, C.sub.1-6 alkylsulphonyl, C.sub.1-6 alkoxysulphinyl, C.sub.1-6 alkoxysulphonyl, C.sub.1-6 alkylcarbonylamino, C.sub.1-6 alkoxycarbonylamino, C.sub.1-6 alkyl-thiocarbonyl, C.sub.1-6 alkoxy-thiocarbonyl, C.sub.1-6 alkyl-thiocarbonyloxy, 1-mercapto C.sub.2-7 alkyl, formyl, or aminosulphinyl, aminosulphonyl or aminocarbonyl, the amino moiety being optionally substituted by one or two C.sub.1-6 alkyl groups, or C.sub.1-6 alkylsulphinylamino, C.sub.1-6 alkylsulphonylamino, C.sub.1-6 alkoxysulphinylamino or C.sub.1-6 alkoxysulphonylamino, or ethylenyl terminally substituted by C.sub.1-6 alkylcarbonyl, nitro or cyano, or --C(C.sub.1-6 alkyl(NOH or --C(C.sub.1-6 alkyl)NNH.sub.2, or one of R.sub.1 and R.sub.Type: GrantFiled: October 21, 1987Date of Patent: May 16, 1989Assignee: Beecham Group p.l.c.Inventors: Frederick Cassidy, Erol A. Faruk
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Patent number: 4826977Abstract: A series of novel photochromic spiropyrans are disclosed in which a spiro-adamantane group is introduced into the 2-position of the benzopyran or naphthopyran ring. The spiropyran compounds of the invention exhibit heliochromic properties, i.e. they color in sunlight and fade rapidly at ambient temperatures in the absence of U.V. light, making them good candidates for use in the manufacture of sunglasses. The invention includes lenses which darken in sunlight and incorporate the novel spiropyrans and a process for the preparation of the spiropyran compounds.Type: GrantFiled: May 15, 1987Date of Patent: May 2, 1989Assignee: The Plessey Company plcInventors: Harry G. Heller, Stephen N. Oliver, John Whittall, Ian Tomlinson
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Patent number: 4820840Abstract: An improved process for producing fluorene compounds of the following formula (II) is disclosed: ##STR1## (wherein R.sub.1, R.sub.2 and R.sub.3 are independently a hydrogen atom, an alkylamino group, a dialkylamino group, a pyrrolidino group or a piperdino group; X and Y are independently a carbon atom or a nitrogen atom; and with the proviso that R.sub.1 and R.sub.2 are not hydrogen atoms simultaneously). The process comprises reacting a lactone compound of the formula (I) (variables being defined as in formula (II) ) ##STR2## with a mixture of an aluminum halide, a carbonyl compound, and a hydroxy bearing compound.Type: GrantFiled: January 22, 1988Date of Patent: April 11, 1989Assignee: Appleton Papers Inc.Inventors: Seishi Ikegami, Satoshi Nakao
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Patent number: 4795811Abstract: A process for converting 6-carboxy to 6-hydroxymethyl mevinolin analogs and novel intermediates formed in this process are disclosed.Type: GrantFiled: June 22, 1987Date of Patent: January 3, 1989Assignee: Merck & Co., Inc.Inventors: Samuel L. Graham, Thomas H. Scholz
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Patent number: 4794069Abstract: Spirobenzanthracene phthalide compounds are disclosed of the formula (I) ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 independently represent C.sub.1 -C.sub.8 alkyl optionally substituted by C.sub.1 -C.sub.5 alkoxy; C.sub.5 or C.sub.6 cycloalkyl; or aralkyl or aryl optionally substituted by C.sub.1 -C.sub.5 alkyl or C.sub.1 -C.sub.5 alkoxy, and R.sup.1 and R.sup.2, R.sup.3 and R.sup.4, and R.sup.5 and R.sup.6 taken together with the nitrogen atom to which they are attached, may form pyrrolidino, piperidino or morpholino ring, and R.sup.7, R.sup.8, R.sup.9 and R.sup.10 independently represent hydrogen, C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkoxy or trifluoromethyl. The compounds are used, together with a developer, in color for materials such as pressure-sensitive copying papers, heat-sensitive recording papers and the like.Type: GrantFiled: July 14, 1987Date of Patent: December 27, 1988Assignee: Shin Nisso Kako Co., Ltd.Inventors: Yutaka Ohnishi, Shinji Yoshinaka, Toshiyuki Tanaka, Minoru Koguchi, Takeo Obitsu
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Patent number: 4794190Abstract: Alpha-(4-maleimidophenyl)-alpha'-(4-isomaleimidophenyl) diisopropyl benzene, as a novel composition of matter. The compound, which may be used as a component of curable thermoset resins or as a unique, difunctional synthesis intermediate having non-symmetrical reactivity, may be prepared from the corresponding bis-maleamic acid by dehydrating at or below ordinary, ambient temperatures, using acetic anhydride or a similar dehydrating agent.Type: GrantFiled: January 28, 1987Date of Patent: December 27, 1988Assignee: Amoco CorporationInventors: Linda A. Domeier, Elke M. Clark
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Patent number: 4772722Abstract: Disclosed are nadimido-substituted cyclophosphazene derivatives and thermosets thereof. The thermosets are useful as high temperature, flame resistant matrices for composites and as metal adhesives.Type: GrantFiled: September 10, 1986Date of Patent: September 20, 1988Assignee: Hercules IncorporatedInventor: Alexander Lukacs, III
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Patent number: 4737493Abstract: Substituted phenoxy-, 1-, and 2-naphthalenyloxy-, indenyl-, indolyl-, benzofuranyl-, and benzo[b]thiofuranylcarboxamides of 7,8-(substituted-diamino)-1-oxaspiro[4.5]decanes are useful as analgesic agents.A method of making the compounds, pharmaceutical compositions employing the compounds, and a method of alleviating pain in warm-blooded animals are also disclosed.Type: GrantFiled: June 9, 1986Date of Patent: April 12, 1988Assignee: Warner-Lambert CompanyInventor: David C. Horwell
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Patent number: 4719224Abstract: Novel optically active isomers or racemic mixtures of thiophene acetic acid derivatives of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms, Y is selected from the group consisting of --OR.sub.2 and ##STR2## R.sub.2 is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms and ##STR3## n is an integer from 2 to 5, X' and X" are individually selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms or taken together with the nitrogen atom form an optionally unsaturated heterocycle of 5 to 6 ring members, R.sub.3 and R.sub.4 are individually selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms and their non-toxic, pharmaceutically acceptable salts with acids and bases having a good analgesic and anti-inflammatory activity and inhibition of 5-lipoxygenase and cyclooxygenase, a process and intermediates for their preparation.Type: GrantFiled: March 6, 1986Date of Patent: January 12, 1988Assignee: Roussel UclafInventors: Francois Clemence, Odile Le Martret, Francoise Delevallee
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Patent number: 4687779Abstract: Compounds of formula (I): ##STR1## wherein: either one of R.sub.1 and R.sub.2 is hydrogen and the other is selected from C.sub.1-6 alkylcarbonyl, C.sub.1-6 alkoxycarbonyl, C.sub.1-6 alkylcarbonyloxy, C.sub.1-6 alkylhydroxymethyl, nitro, cyano, chloro, trifluoromethyl, C.sub.1-6 alkylsulphinyl, C.sub.1-6 alkylsulphonyl, C.sub.1-6 alkoxysulphinyl,C.sub.1-6 alkoxysulphonyl, C.sub.1-6 alkylcarbonylamino, C.sub.1-6 alkoxycarbonylamino, C.sub.1-6 alkyl-thiocarbonyl, C.sub.1-6 alkoxy-thiocarbonyl, C.sub.1-6 alkyl-thiocarbonyloxy, C.sub.1-6 alkyl-thiolmethyl, formyl or aminosulphinyl, aminosulphonyl or aminocarbonyl, the amino moiety being optionally substituted by one or two C.sub.1-6 alkyl groups, or C.sub.1-6 alkylsulphinylamino, C.sub.1-6 alkylsulphonylamino C.sub.1-6 alkoxysulphinylamino or C.sub.1-6 alkoxysulphonylamino or ethylenyl terminally substituted by C.sub.1-6 alkylcarbonyl, nitro or cyano, or --C(C.sub.1-6 alkyl)NOH or --C(C.sub.1-6 alkyl)NNH.sub.2, or one of R.sub.1 and R.sub.2 is nitro, cyano or C.Type: GrantFiled: August 29, 1984Date of Patent: August 18, 1987Assignee: Beecham Group p.l.c.Inventor: John M. Evans
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Patent number: 4685783Abstract: A series of photochromic compounds are disclosed which have the property of undergoing a reversible color change when exposed to unfiltered sunlight and reverting to their original color in the absence of U.V. light at room temperature. These compounds have the general formula: ##STR1## represents an adamantylidene or a substituted adamantylidene group;R.sub.1 represents hydrogen, alkyl, aryl, aralkyl or a heterocyclic group,X represents oxygen or > NR.sub.2, in which R.sub.2 is hydrogen, aryl, alkyl or aralkyl and ##STR2## represents an aromatic group, an unsaturated heterocyclic group or a benzannelated heterocyclic group.The photochromic compounds of the invention are useful in the manufacture of photoreactive lenses, particularly plastic lenses.Type: GrantFiled: September 5, 1984Date of Patent: August 11, 1987Assignee: The Plessey Company P.L.C.Inventors: Harold H. Heller, Stephen N. Oliver, John Whittal, William Johncock, Paul J. Darcy, Clive Trundle
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Patent number: 4659737Abstract: Substituted benzopyrans of the formula ##STR1## in which --A-- is a single or double bond,X is a direct bond, optionally substituted methylene, oxygen or optionally substituted --NH--, and the various other radicals can have various meanings,or pharmaceutically acceptable addition salts thereof, which possess anti-hypertensive activity.Type: GrantFiled: March 25, 1985Date of Patent: April 21, 1987Assignee: Bayer AktiengesellschaftInventors: Hans-Joachim Kabbe, Ulrich Niewohner, Arno Widdig, Andreas Knorr, Bernward Garthoff, Stanislav Kazda
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Patent number: H642Abstract: Compounds of the formula ##STR1## wherein X is various imino or amino acids or esters are disclosed. These compounds possess angiotensin converting enzyme inhibition activity and depending upon the definition of X also possess enkephalinase inhibition activity.Type: GrantFiled: August 20, 1984Date of Patent: June 6, 1989Assignee: E. R. Squibb & Sons, Inc.Inventors: David Floyd, Melanie J. Loots