Polycyclo Ring System In A Substituent E Patents (Class 564/222)
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Patent number: 5470977Abstract: The present invention provides novel ring-substituted 2-amino-1,2,3,4-tetrahydronaphthalenes, 3-aminochromanes, and 3-aminothiochromanes, including their corresponding sulfoxides and sulfones, which ring-substituted compounds exhibit agonist activity at the serotonin 1A receptor.Type: GrantFiled: March 14, 1995Date of Patent: November 28, 1995Assignee: Eli Lilly and CompanyInventors: John M. Schaus, Craig S. Hoechstetter, Diane Huser, Charles J. Paget, Robert D. Titus
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Patent number: 5463126Abstract: The invention provides the substantially geometrically pure cis-stereoisomeric form of a compound of formula (I) and the substantially geometrically and optically pure cis-stereoisomeric form of a compound of formula (II): ##STR1## wherein R.sup.1 is H or C.sub.1 -C.sub.4 alkyl, together with processes for their preparation. The compounds are intermediates for the preparation of the antidepressant agent known as sertraline.Type: GrantFiled: January 10, 1994Date of Patent: October 31, 1995Assignee: Pfizer Inc.Inventor: Michael T. Williams
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Patent number: 5442116Abstract: The invention provides the substantially geometrically and optically pure trans-stereoisomeric form of a compound of formula (I): ##STR1## wherein R.sup.1 is H or C.sub.1 -C.sub.4 alkyl, together with processes for its preparation. The compounds are intermediates for the preparation of the antidepressant agent known as sertraline.Type: GrantFiled: January 10, 1994Date of Patent: August 15, 1995Assignee: Pfizer Inc.Inventors: Willard M. Welch, Michael T. Williams
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Ring-substituted 2-amino-1,2,3,4-tetra-hydronaphthalenes, 3-aminochromanes, and 3-aminothiochromanes
Patent number: 5426229Abstract: The present invention provides novel ring-substituted 2-amino-1,2,3,4-tetrahydronaphthalenes, 3-aminochromanes, and 3-aminothiochromanes, including their corresponding sulfoxides and sulfones, which ring-substituted compounds exhibit agonist activity at the serotonin 1A receptor.Type: GrantFiled: December 16, 1993Date of Patent: June 20, 1995Assignee: Eli Lilly and CompanyInventors: John M. Schaus, Craig S. Hoechstetter, Diane Huser, Charles J. Paget, Robert D. Titus -
Patent number: 5248823Abstract: Diphenylheteroalkyl derivatives of the formula I ##STR1## where A and R.sup.1 -R.sup.6 have the meanings specified in the description, and the preparation thereof are described.The substances are suitable for controlling diseases and as cosmetic agents.Type: GrantFiled: December 4, 1992Date of Patent: September 28, 1993Assignee: BASF AktiengesellschaftInventors: Bernd Janssen, Hans-Heiner Wuest
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Patent number: 5225595Abstract: Sulfonyl compounds of the formula ##STR1## where Ar is the radical of a benzene or naphthalene ring,R.sup.1 and R.sup.2 are each hydrogen, substituted or unsubstituted C.sub.1 -C.sub.4 -alkyl, substituted or unsubstituted phenyl, C.sub.1 -C.sub.4 -alkoxy, carboxyl, C.sub.1 -C.sub.4 -alkoxycarbonyl, cyano, halogen or hydroxysulfonyl,R.sup.3 is nitro, amino, C.sub.1 -C.sub.4 -alkanoylamino or benzoylamino, andR.sup.4 is a radical of the formula ##STR2## where X.sup.1, X.sup.2 and X.sup.3 are each hydrogen, substituted or unsubstituted C.sub.1 -C.sub.4 -alkyl or substituted or unsubstituted phenyl, andX.sup.4 is a group which is detachable under alkaline conditions,either in the free form or in the form of their salts, are useful for synthesizing reactive dyes.Type: GrantFiled: November 4, 1992Date of Patent: July 6, 1993Assignee: BASF AktiengesellschaftInventors: Bernd Siegel, Claus Marschner, Manfred Patsch
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Patent number: 5225601Abstract: Abstract of the Disclosure: Diphenylheteroalkyl derivatives of the formula I ##STR1## where A and R.sup.1 -R.sup.6 have the meanings specified in the description, and the preparation thereof are described.The substances are suitable for controlling diseases and as cosmetic agents.Type: GrantFiled: October 31, 1991Date of Patent: July 6, 1993Assignee: BASF AktiengesellschaftInventors: Bernd Janssen, Hans-Heiner Wuest
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Patent number: 5196454Abstract: The invention relates to novel 2,5-diaminotetralines of the formula: ##STR1## wherein R1, R2, R3 and R4 are defined herein, processes for preparing them and their use in pharmaceutical compositions. The novel 2,5-diaminotetralines are useful in treating diseases caused by disorders of the dopaminergic systems.Type: GrantFiled: June 15, 1990Date of Patent: March 23, 1993Assignee: Boehringer Ingelheim KGInventors: Matthias Grauert, Herbert Merz, Joachim Mierau, Gunter Schingnitz, Claus Schneider
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Patent number: 5189065Abstract: The use of products of formula (I) is described, wherein X and Y represent hydrogen, hydroxy or alkoxy; and R.sub.1 and R.sub.2 represent H, alkyl, alkenyl or alkynyl, arylalkyl, acyl or R.sub.1 and R.sub.2 together with nitrogen form a heterocycle for preparing an antitumoral drug.Type: GrantFiled: October 17, 1991Date of Patent: February 23, 1993Assignee: Roussel UclafInventors: Jorg Czech, Hans H. Sedlacek, Lucien Nedelec, Jacques Guillaume, Christian Marchandeau
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Patent number: 5153227Abstract: The invention concerns novel pharmaceutical compositions for use in the treatment of certain complications of diabetes and galactosemia and which contain a nitromethane derivative (or its non-toxic salt) as active ingredient. The nitromethane derivatives are inhibitors of the enzyme aldose reductase. Many of the inhibitors are novel and are provided, together with processes for their manufacture and use, as further features of the invention.Type: GrantFiled: February 6, 1989Date of Patent: October 6, 1992Assignee: Imperial Chemical Industries PLCInventors: Steven P. Brown, Anthony L. Cooper, Jethro L. Longridge, Jeffrey J. Morris, John Preston
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Patent number: 5128479Abstract: Oxidized diphenylheteroalkanes of the formula I ##STR1## where R.sup.1 to R.sup.6 and A have the meanings specified in the description, and the preparation thereof are described. The substances are suitable for controlling diseases and as cosmetic agents.Type: GrantFiled: January 29, 1990Date of Patent: July 7, 1992Assignee: BASF AktiengesellschaftInventors: Bernd Janssen, Hans-Heiner Wuest
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Patent number: 5114975Abstract: The invention relates to novel substituted aryloxyphenylthioureas, aryloxyphenylisothioureas and aryloxyphenylcarobodiimides of formula I ##STR1## wherein R.sub.1 is C.sub.1 -C.sub.12 alkyl, unsubstituted or substituted by one or more halogen atoms and/or C.sub.1 -C.sub.6 alkoxy groups; C.sub.3 -C.sub.8 cycloalkyl, unsubstituted or substituted by one or more C.sub.1 -C.sub.3 alkyl groups; or C.sub.3 -C.sub.8 cycloalkyl-C.sub.1 -C.sub.4 alkyl,R.sub.2 and R.sub.3 are each C.sub.1 -C.sub.5 alkyl or C.sub.5 -C.sub.6 cycloalkyl,R.sub.4 is hydrogen, methyl or --CHO,R.sub.5 is halogen; C.sub.1 -C.sub.4 alkyl, unsubstituted or substituted by one or more halogen atoms; C.sub.1 -C.sub.4 alkoxy, unsubstituted or substituted by one or more halogen atoms; or is a --CH.dbd.CH).sub.2, --CH.sub.2).sub.3 or --CH.sub.2).sub.4 bridge in 2,3- or 3,4-position,n is 0, 1, 2, 3 or 4,Z is --NH--CS--NH--, --N.dbd.C(SR.sub.6)--NH-- or --N.dbd.C.dbd.N--; andR.sub.6 is C.sub.1 -C.sub.Type: GrantFiled: April 3, 1991Date of Patent: May 19, 1992Assignee: Ciba-Geigy CorporationInventors: Manfred Boger, Jozef Drabek, Josef Ehrenfreund
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Patent number: 5087743Abstract: Diphenylheteroalkyl derivatives of the formula I ##STR1## where A and R.sup.1 -R.sup.6 have the meanings specified in the description, and the preparation thereof are described.The substances are suitable for controlling diseases and as cosmetic agents.Type: GrantFiled: January 23, 1990Date of Patent: February 11, 1992Assignee: BASF AktiengesellschaftInventors: Bernd Janssen, Hans-Heiner Wuest
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Patent number: 5071875Abstract: The present invention relates generally to compounds having melatonin receptor activities and in particular to substituted 2-amidotetralin derivatives; to pharmaceutical preparations comprising such compounds; and to methods for using these compounds as therapeutic and diagnostic reagents.Type: GrantFiled: September 25, 1989Date of Patent: December 10, 1991Assignee: Northwestern UniversityInventors: Alan S. Horn, Margarita L. Dubocovich
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Patent number: 5053430Abstract: Novel compounds having the general formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined herein. These compounds are useful in the treatment of schizophrenia.Type: GrantFiled: September 22, 1989Date of Patent: October 1, 1991Assignee: Boehringer Ingelheim KGInventors: Matthias Grauert, Herbert Merz, Joachim Mierau, Gunter Schingnitz, Claus Schneider
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Patent number: 5026730Abstract: The invention relates to novel substituted anilinophenylthioureas, anilinophenylisothioureas and anilinophenylcarbodiimides of formula I ##STR1## wherein R.sub.1 is C.sub.1 -C.sub.12 alkyl, unsubstituted or substituted by one or more halogen atoms and/or C.sub.1 -C.sub.6 alkoxy groups; C.sub.3 -C.sub.8 cycloalkyl, unsubstituted or substituted by one or more C.sub.1 -C.sub.3 alkyl groups; or C.sub.3 -C.sub.8 cycloalkyl-C.sub.1 -C.sub.4 alkyl,R.sub.2 and R.sub.3 are each C.sub.1 -C.sub.5 alkyl or C.sub.5 -C.sub.6 cycloalkyl,R.sub.4 is hydrogen, methyl or --CHO,R.sub.5 is halogen; C.sub.1 -C.sub.4 alkyl, unsubstituted or substituted by one or more halogen atoms; C.sub.1 -C.sub.4 alkoxy, unsubstituted or substituted by one or more halogen atoms; or is a --CH.dbd.CH--.sub.2, --CH.sub.2--3 or --CH.sub.2--4 bridge in 2,3- or 3,4-position,n is 0, 1, 2, 3 or 4,Z is --NH--CS--NH--, --N.dbd.C(SR.sub.6)--NH-- or --N.dbd.C.dbd.N--; andR.sub.6 is C.sub.1 -C.sub.Type: GrantFiled: August 11, 1988Date of Patent: June 25, 1991Assignee: Ciba-Geigy CorporationInventors: Manfred Boger, Jozef Drabek, Josef Ehrenfreund
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Patent number: 5021414Abstract: A phenol derivative of the formulaNU--A--X--R.sup.1wherein NU is a defined bis-phenolic nucleus including a hydroxyphenyl-hydroxynaphthyl; hydroxyphenyl-hydroxyindanyl, hydroxyphenyl-hydroxybenzothienyl or di-hydroxyphenyl-ethylene or vinylene nucleus;wherein A is alkylene, alkenylene or alkynylene which may be interrupted by phenylene or other linkages,wherein R.sup.1 is hydrogen, or alkyl, alkenyl, cycloalkyl, halogenoalkyl, aryl or arylalkyl, or R.sup.1 is joined to R.sup.2, and wherein X is --CONR.sup.2 --, --CSNR.sup.2 --, --NR.sup.12 CO--, --NR.sup.12 CS--, --NR.sup.12 CONR.sup.2 --, ##STR1## --SO.sub.2 NR.sup.2 -- or --CO--, or, when R.sup.1 is not hydrogen, is --NR.sup.12 COO--, --S--, --SO-- or --SO.sub.2 --,wherein R.sup.2 is hydrogen or alkyl, or R.sup.1 and R.sup.2 together form alkylene;wherein R.sup.12 is hydrogen or alkyl, and wherein R.sup.22 is hydrogen, cyano or nitro;or a salt thereof when appropriate.Type: GrantFiled: December 18, 1989Date of Patent: June 4, 1991Assignee: Imperial Chemical Industries PLCInventors: William R. Pilgrim, Derek W. Young, Brian S. Tait, Graham C. Crawley, Philip N. Edwards, George B. Hill
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Patent number: 4975461Abstract: p-Aminophenols are provided having the structure ##STR1## wherein m is 0, 1 or 2; n is 0, 1, 2 or 3; R.sup.1 and R.sup.2 may be the same or different and are H, hydroxy or alkoxy; R.sup.3 is H, lower alkyl, alkanoyl or aroyl and R.sup.4 is H, lower alkyl or alkanoyl, and including acid-addition salts thereof.These compounds are useful as inhibitors of leukotriene production and as such are useful as antiallergy, anti-inflammatory and anti-psoriatic agents.Type: GrantFiled: June 19, 1986Date of Patent: December 4, 1990Assignee: E. R. Squibb & Sons, Inc.Inventor: Raj N. Misra
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Patent number: 4922016Abstract: N-(sulfonylmethyl)formamides are obtained by reacting a sulfinic acid, formaldehyde and formamide in the presence of a second acid and a controlled amount of water. The formamides can be converted to the corresponding sulfonylmethylisocyanides.Type: GrantFiled: July 26, 1989Date of Patent: May 1, 1990Assignee: Gist-Brocades N.V.Inventor: Nicolaas C. M. E. Barendse
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Patent number: 4889924Abstract: A bisazo compound having good electrophotographic properties is disclosed, which is represented by formula (I) ##STR1## wherein X represents a hydrogen atom, a chlorine atom or a nitro group. A process for producing the bisazo compound is also disclosed.Type: GrantFiled: October 2, 1987Date of Patent: December 26, 1989Assignee: Fuji Xerox Co., Ltd.Inventors: Yutaka Akasaki, Akihiko Tokita, Kaoru Torikoshi, Akira Imai, Touru Ishii
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Patent number: 4885314Abstract: Novel 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors which are useful as antihypercholesterolemic agents and are represented by the following general structural formulae (I) or (II): ##STR1## and pharmaceutically acceptable salts thereof the compounds of the formula (II) in which R.sup.1 is hydrogen are disclosed.Type: GrantFiled: September 1, 1988Date of Patent: December 5, 1989Assignee: Merck & Co., Inc.Inventors: Kamlesh P. Vyas, Hanumath P. Kari
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Patent number: 4792628Abstract: Indane derivatives and their salts represented by the general formula (1), ##STR1## wherein R.sup.1 is an amino group which may have lower alkyl groups as the substituents, a hydroxylimino group, an alkanoylamino group having 1 to 10 carbon atoms which may have halogen atoms as the substituents, a lower alkylsulfonylamino group, a phenylsulfonylamino group which may have lower alkyl groups as the substituents on the phenyl ring, a benzoylamino group having lower alkyl groups as the substituents on the phenyl ring, and a phenyl-lower alkylamino group having a hydroxyl groups or a lower alkyl groups as the substituents on the phenyl ring, R.sup.2 is a hydrogen atom, a lower alkyl group, a halogen atom, a nitro group, an amino group, an amino-lower alkyl group, a lower alkanoylamino group, a lower alkanoylamino-lower alkyl group which may have halogen atoms as the substituents, a lower alkylthio group, a 1-piperidinesulfonyl group, or a lower alkenyl group; R.sup.Type: GrantFiled: April 16, 1987Date of Patent: December 20, 1988Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Yasuo Oshiro, Hiraki Ueda, Kazuyuki Nakagawa
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Patent number: 4755511Abstract: This invention relates to tricyclic pyridazinone compounds, pharmaceutical compositions containing the compounds, and a method of stimulating cardiac activity in a mammal by administering an effective amount of the compound. A compound of the invention is 7-carboxamido-4,4a-dihydro-4a-methyl-[5H]-indeno[1,2-c]-pyridazin-3[2H]-on e.Type: GrantFiled: September 22, 1987Date of Patent: July 5, 1988Assignee: Smith Kline & French Laboratories LimitedInventor: Brian H. Warrington
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Patent number: 4754066Abstract: Compounds corresponding to the formula ##STR1## wherein R.sup.1 and R.sup.2 represent H or C.sub.1 -C.sub.4 -alkyl,R.sup.3 represents H or CH.sub.3,R.sup.4 represents C.sub.7 -C.sub.20 -aralkyl,n represents 1 or 2, andm represents an integer of from 1 to 12,are suitable as ageing protecting agents for polymers and in particular for rubbers which are non-extractable in this form and may be added to polymers.Type: GrantFiled: March 26, 1986Date of Patent: June 28, 1988Assignee: Bayer AktiengesellschaftInventors: Hans-Josef Buysch, Zsolt Szentivanyi, Josef Witte
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Patent number: 4751240Abstract: A phenol derivative of the formulaNU--A--X--R.sup.1wherein NU is a defined phenolic nucleus including a phenyl-hydroxynaphthyl; hydroxyphenyl-naphthyl; phenyl-hydroxyindanyl, phenyl-hydroxybenzothienyl or mono-hydroxyphenyl-ethylene or vinylene nucleus; wherein A is alkylene, alkenylene or alkynylene which may be interrupted by phenylene or other linkages, wherein R.sup.1 is hydrogen, or alkyl, alkenyl, alkynyl, cycloalkyl, halogenoalkyl, alkoxyalkyl, halogenoalkoxyalkyl, aryl or arylalkyl, or R.sup.1 is joined to R.sup.2, and wherein X is --CONR.sup.2 --, --CSNR.sup.2 --, --NR.sup.12 CO--, --NR.sup.12 CS--, --NR.sup.12 CONR.sup.2 --, ##STR1## --SO.sub.2 NR.sup.2 --or --CO--, or, when R.sup.1 is not hydrogen, is --NR.sup.12 COO--, --(PO)R.sup.2 13 , --S--, --SO--or --SO.sub.2 --, wherein R.sup.2 is hydrogen or alkyl, or R.sup.1 and R.sup.2 together form alkylene; wherein R.sup.12 is hydrogen or alkyl, and wherein R.sup.22 is hydrogen, cyano or nitro; or a salt thereof when appropriate.Type: GrantFiled: April 24, 1985Date of Patent: June 14, 1988Assignee: Imperial Chemical Industries PLCInventors: Jean Bowler, Graham C. Crawley, Philip N. Edwards, Alasdair T. Glen, Michael S. Large, Brian S. Tait
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Patent number: 4692463Abstract: The present invention describes the finding of potent antiinflammatory properties in 2,3-didemethylcolchicine and its analogs.Type: GrantFiled: November 29, 1985Date of Patent: September 8, 1987Assignee: The United States of America as represented by the Department of Health and Human ServicesInventor: Arnold Brossi
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Patent number: 4692447Abstract: The tricyclic dihydropyridazinone derivatives having formula I ##STR1## are endowed with interesting hypotensive, vasodilating, antiaggregant, antithrombotic and cytoprotective properties and are therefore useful in human or veterinary medicine.Type: GrantFiled: July 22, 1985Date of Patent: September 8, 1987Assignee: Boehringer Biochemia Robin, S.p.A.Inventors: Giorgio Cignarella, Carmelo A. Gandolfi, Odoardo Tofanetti, Piervitto Cipolla, Sergio Tognella
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Patent number: 4642373Abstract: 1,2,3,4,4a,4b,5,6,7,8,8a,12b-Dodecahydro-7-(oxo, hydroxy or amino)-9-hydroxy-11-(alkyl, alkoxy or alkoxyalkyl)triphenylenes, 2,3,3a,3b,4,5,6,7,7a,11b-decahydro-6-(oxo, hydroxy or amino)-8-hydroxy-10-(alkyl, alkoxy or alkoxyalkyl)-1H-cyclopenta[1]-phenanthrenes, 2,3,4,4a,4b,5,6,7,8,8a-decahydro-7-(oxo, hydroxy or amino)-9-hydroxy-11-(alkyl, alkoxy, alkoxyalkyl, aralkyl, aralkoxy, aryloxyalkyl or aralkoxyalkyl)-1H-pyrido[1,2-f]phenanthridines, and 1,2,3,3a,3b,4,5,6,7,7a-decahydro-6-(oxo, hydroxy or amino)-8-hydroxy-10-(alkyl, alkoxy or alkoxyalkyl)pyrrolo[1,2-f]phenanthridines and derivatives are valuable as central nervous system active agents or as intermediates to compounds having such activity.Type: GrantFiled: July 6, 1984Date of Patent: February 10, 1987Assignee: Pfizer Inc.Inventors: James F. Eggler, Michael R. Johnson, Lawrence S. Melvin, Jr.
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Patent number: 4604128Abstract: The invention concerns novel compounds of the formula I ##STR1## wherein: m is an integer selected from 1 to 4;n is zero or an integer selected from 1 to 4;X are selected from halogen, nitro, cyano, alkyl, substituted alkyl, hydroxy, alkoxy, alkylthio, sulfamoyl, substituted sulfamoyl, amino, substituted amino, the group --(CH.sub.2).sub.p C(.dbd.A)Z in which p is zero or one A is oxygen or sulfur, and Z is hydrogen, hydroxy, alkoxy, alkylthio, alkyl, substituted alkyl, amino or substituted amino, the group --NHC(.dbd.B)NR.sup.7 R.sup.8 in which B is oxygen or sulfur and R.sup.7 and R.sup.8 are hydrogen or alkyl;R.sup.1 is selected from hydrogen, acyl and an inorganic or organic cation;R.sup.2 is selected from alkyl, substituted alkyl, alkenyl, haloalkenyl, alkynyl and haloalkynyl;R.sup.3 is selected from alkyl, fluoroalkyl, alkenyl, alkynyl, and phenyl; andR.sup.4 is selected from hydrogen, halogen, alkyl, cyano and alkoxycarbonyl.Type: GrantFiled: September 10, 1985Date of Patent: August 5, 1986Assignee: ICI Australia LimitedInventors: Keith G. Watson, John D. Wishart, Graeme J. Farquharson, Graham J. Bird, Lindsay E. Cross
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Patent number: 4602032Abstract: A 2-alkyl-9,10-dioxy-4,5,5a,6-tetrahydro-dibenz[cd,f]indole or an acid addition salt thereof is a useful anti-parkinson agent.Type: GrantFiled: December 19, 1984Date of Patent: July 22, 1986Assignee: Sandoz Ltd.Inventor: Rudolf K. A. Giger
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Patent number: 4540806Abstract: Benzocycloalkane amine derivatives and their non-toxic acid addition salts as novel analgesic agents.Type: GrantFiled: December 22, 1983Date of Patent: September 10, 1985Assignee: American Home Products CorporationInventors: Meier E. Freed, Magid A. Abou-Gharbia
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Patent number: 4473704Abstract: 1,2,3,4,4a,4b,5,6,7,8,8a,12b-Dodecahydro-7-(oxo, hydroxy or amino)-9-hydroxy-11-(alkyl, alkoxy or alkoxyalkyl)triphenylenes, 2,3,3a,3b,4,5,6,7,7a,11b-decahydro-6-(oxo, hydroxy or amino)-8-hydroxy-10-(alkyl, alkoxy or alkoxyalkyl)-1H-cyclopenta[1]phenanthrenes, 2,3,4,4a,4b,5,6,7,8,8a-decahydro-7-(oxo, hydroxy or amino)-9-hydroxy-11-(alkyl, alkoxy, alkoxyalkyl, aralkyl, aralkoxy, aryloxyalkyl or aralkoxyalkyl)-1H-pyrido[1,2-f]phenanthridines, and 1,2,3,3a,3b,4,5,6,7,7a-decahydro-6-(oxo, hydroxy or amino)-8-hydroxy-10-(alkyl, alkoxy or alkoxyalkyl)pyrrolo[1,2-f]phenanthridines and derivatives are valuable as central nervous system active agents or as intermediates to compounds having such activity.Type: GrantFiled: March 16, 1982Date of Patent: September 25, 1984Assignee: Pfizer Inc.Inventors: James F. Eggler, Michael R. Johnson, Lawrence S. Melvin, Jr.
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Patent number: 4473586Abstract: Disclosed herein are 1-aminoalkyl-3,4-dihydronaphthalenes represented by the formula ##STR1## wherein n is 1 or 2; R, R.sub.1, and R.sub.2 are independently selected from hydrogen, hydroxy, loweralkoxy of 1 to 3 carbon atoms, loweralkenyloxy of 1 to 3 carbon atoms, thiomethyl, halo, or ##STR2## wherein R.sub.5 and R.sub.6 are independently selected from hydrogen, loweracyl of 1 to 4 carbon atoms or sulfonyl of the formula ##STR3## wherein R.sub.7 is loweralkyl of 1 to 4 carbon atoms; or R and R.sub.1, or R.sub.1 and R.sub.2 can be taken together to form a methylenedioxy or ethylenedioxy bridge; with the proviso that at least one of R, R.sub.1 or R.sub.2 must be other than hydrogen; and R.sub.3 and R.sub.4 are independently selected from hydrogen; loweralkyl of 1 to 4 carbon atoms; halo-substituted loweralkyl of 1 to 4 carbon atoms; arylalkyl of the formula ##STR4## wherein m is 0, 1 or 2, p is 0 or 1, R.sub.8 is hydrogen or loweralkyl of 1 to 4 carbon atoms and R.sub.9 and R.sub.Type: GrantFiled: May 3, 1982Date of Patent: September 25, 1984Assignee: Abbott LaboratoriesInventors: John F. Debernardis, David L. Arendsen, Martin Winn
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Patent number: 4442126Abstract: New compounds of the formula: ##STR1## wherein R.sub.1 represents a hydrogen atom or an alkanoyl group containing from 1 to 4 carbon atoms, R.sub.2 and R.sub.3 each represent a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group, and R.sub.4 represents a hydroxy or methoxy group in the 6-position or 7-position, have been found to be useful in therapy, and more particularly in the treatment of cardiovascular diseases and Parkinson's disease.Type: GrantFiled: September 15, 1982Date of Patent: April 10, 1984Assignee: SynthelaboInventors: Nigel R. A. Beeley, Gerard Cremer, Michael J. Dimsdale, Philippe Manoury
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Patent number: 4435426Abstract: The present invention relates to novel products, responding to general formula: ##STR1## in which R.sub.1 and R.sub.2 taken together represent an atom of oxygen .dbd.O or R.sub.1 represents hydrogen and R.sub.2 represents an OH radical, R.sub.3 designates an atom of hydrogen or a straight or branched alkyl radical, or an alkynyl group having from 1 to 6 atoms of carbon, R.sub.4 represents a straight or branched alkyl radical having from 1 to 6 atoms of carbon, R.sub.5 designates an atom of hydrogen, an alkyl group having from 1 to 4 atoms of carbon or an acylamine group and n=3 or 4; as well as to the acid addition salts of said products, to a process for preparing said products and to drugs, particularly active on the cardiovascular system, containing at least one of said products.Type: GrantFiled: May 25, 1982Date of Patent: March 6, 1984Assignee: Societe Anonyme dite: SanofiInventors: Henri Demarne, Jean Wagnon
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Patent number: 4405358Abstract: Aralkylaniline derivatives of the general formula ##STR1## where R is alkoxy, cycloalkoxy, alkenyloxy, alkynyloxy, cyanoalkoxy, haloalkoxy, alkylthio, alkenylthio or alkynylthio or unsubstituted or substituted alkyl, cycloalkyl, alkenyl or alkynyl, Y is hydrogen, alkyl, halogen, alkoxy or haloalkyl, A is unsubstituted or substituted alkylene, Z is hydrogen, alkyl, haloalkyl, alkoxyalkyl, cycloalkyl, aralkyl, aryl, aryloxy, halogen, a C.sub.4 H.sub.4 -chain which is fused to the benzene radical to form an unsubstituted or substituted naphthyl radical, alkoxy, haloalkoxy, alkylthio, thiocyanato, cyano, ##STR2## R' and R" each, independently of one another, being hydrogen, alkyl, alkoxy, alkylthio, cycloalkyl or unsubstituted or substituted phenyl, and n is an integer from 1 to 4, and herbicides containing these compounds.Type: GrantFiled: May 1, 1981Date of Patent: September 20, 1983Assignee: BASF AktiengesellschaftInventors: Ulrich Schirmer, Wolfgang Rohr, Bruno Wuerzer
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Patent number: 4394314Abstract: A process of reacting a ring carbon atom of an aromatic compound Ar with a compound of the formula H.sub.2 NCH.dbd.NH.sub.2.sup.+ CH.sub.3 CO.sub.2.sup.-, and an anhydride which has the ##STR1## at from 10.degree. to 200.degree. C. and preferably 25.degree. to 40.degree. C. to form a compound of the formula ##STR2## where m is 1, 2 or 3, and A is H or F. In the case where m is 1 the compound ##STR3## can be hydrolyzed to ArCHO.Type: GrantFiled: April 23, 1981Date of Patent: July 19, 1983Assignee: E. I. Du Pont de Nemours and CompanyInventor: Wallace C. Petersen
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Patent number: 4377587Abstract: The invention relates to novel microbicides of the general formula I ##STR1## wherein R is hydrogen or methyl, Ar is a phenyl or .alpha.-naphthyl group which is substituted by NH.sub.2 or NO.sub.2 and further radicals, W is a cyano, ester, alkenyl or alkynyl group, and B is alkyl, alkenyl, cyclopropyl, 2-furyl, 2-tetrahydrofuryl, .beta.-(alkoxy)ethyl, triazolylmethyl, methylsulfonylmethyl, alkoxymethyl, alkenyloxymethyl, alkynyloxymethyl, alkylthiomethyl, alkenylthiomethyl, alkynylthiomethyl, --OSO.sub.2 -alkyl, --OSO.sub.2 NH(alkyl) or --N(alkyl).sub.2. The invention also describes plant protection compositions which contain these compounds, a process for the production of the novel compounds and compositions, and a method of controlling phytopathogenic microorganisms which comprises the use thereof.Type: GrantFiled: July 21, 1981Date of Patent: March 22, 1983Assignee: Ciba-Geigy CorporationInventors: Adolf Hubele, Wolfgang Eckhardt, Peter Riebli
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Patent number: 4320148Abstract: 2-Aminotetralin compounds having 5- and 8- substituents are centrally acting alpha.sub.1 agonists.Type: GrantFiled: November 24, 1980Date of Patent: March 16, 1982Assignee: SmithKline CorporationInventor: Robert M. DeMarinis
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Patent number: 4310693Abstract: o-Aminophenol derivatives are described represented by the formula (I) ##STR1## wherein R represents --NH.sub.2 or --NH--CO--R.sup.6 ; R.sup.1 and R.sup.2 which may be the same or different, each can represent an alkyl group or an aromatic group, or R.sup.1 and R.sup.2 together can form a ring; or R.sup.1, R.sup.2 and R.sup.3 together can form a ring ; R.sup.3 represents hydrogen, an alkyl group or an aromatic group; R.sup.4 can represent an alkyl group or an aromatic group; R.sup.5 can represent an alkyl group, an alkoxy group, an alkylthio group, an arylthio group, a halogen atom or an acylamino group; and n is 0, 1 or 2; R.sup.6 represents an alkyl group or an aromatic group; and R.sup.4 and R.sup.5 together can form a heterocyclic ring, R.sup.1 and R.sup.4 together can form a heterocyclic ring, or R.sup.1 and R.sup.5 together can form a ring; and R.sup.1, R.sup.2, R.sup.3, R.sup.4, and R.sup.5.sub.n have a total of 7 or more carbon atoms.Type: GrantFiled: July 18, 1980Date of Patent: January 12, 1982Assignee: Fuji Photo Film Co., Ltd.Inventors: Shinsaku Fujita, Koichi Koyama, Yoshio Inagaki
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Patent number: 4299984Abstract: The present invention relates to novel biologically active tricyclic compounds of the general formula: ##STR1## and salts thereof, in whichR.sub.1 and R.sub.2 stand for hydrogen, alkyl or alkenyl, an optionally substituted aralkyl group or an acyl group orR.sub.1 +R.sub.2 together with the nitrogen atom represent a heterocyclic 5- or 6-membered ring, andX and Y stand for hydrogen, hydroxy, halogen, alkyl or alkoxy of 1-6 carbon atoms, nitro, trifluoromethyl or an acyloxy group,which compounds have valuable biological activities, particularly anorectic activity.Type: GrantFiled: December 30, 1977Date of Patent: November 10, 1981Assignee: Akzona IncorporatedInventors: Colin L. Hewett, David S. Savage
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Patent number: 4254268Abstract: There is provided an oxidation process using potassium permanganate as oxidizing agent, for the preparation of certain animal growth promoters, namely, N-(4,5,6,7-tetrahydro-7-oxobenzo[b]thien-4-yl)amides, 4,5,6,7-tetrahydro-7-oxobenzo[b]-thien-4-ylureas, N-(1,2,3,4-tetrahydro-4-oxo-1-naphthyl)amides and 1,2,3,4-tetrahydro-4-oxo-1-naphthylureas, said process affording such compounds in markedly improved yields, and being readily suitable for scale-up.Type: GrantFiled: June 22, 1978Date of Patent: March 3, 1981Assignee: American Cyanamid CompanyInventor: Henry L. Strong
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Patent number: 4232158Abstract: 10,11-Dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imines, derivatives and pharmaceutically acceptable salts thereof are useful as antianxiety agents, as muscle relaxants and in the treatment of extrapyramidal disorders such as in Parkinson's disease. They are prepared by treatment of a 5H-dibenzo[a,d]cyclohepten-5-one with ammonia to give the 5-imine, acylation of the imine, treatment of the protected imine with an organolithium to provide the 5-substituted-5-acylamino compound, treatment with acid or base to cause ring closure to a 5-substituted-5,10-acylimino compound followed by removal of the protecting group, either hydrolytically or hydrogenolytically.Type: GrantFiled: June 4, 1979Date of Patent: November 4, 1980Assignee: Merck & Co., Inc.Inventors: Kenneth L. Shepard, Daniel G. Brenner