The Additional Six-membered Hetero Ring Is One Of The Cyclos In A Bicyclo Ring System Patents (Class 544/151)
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Patent number: 4923641Abstract: Highly concentrated stable solutions of color-forming agents of the general formula ##STR1## wherein x denotes hydroxyl, alkoxy, alkenyloxy, aralkoxy, cycloalkoxy, aryloxy, acyloxy, alkylamino, dialkylamino, acylamino, aralkylamino or arylamino andR denotes alkyl, alkenyl or aralkyl,further isocyclic or heterocyclic rings can be fused onto the rings A, B, C and D and the cyclic and acyclic radicals and the rings A, B, C and D can carry further non-ionic substituents which are customary in dyestuff chemistry, or mixtures thereof, in water-insoluble organic solvents from the group comprising optionally chlorinated hydrocarbons, vegetable oils and phthalic acid esters are used for the preparation of pressure-sensitive recording materials.Type: GrantFiled: September 20, 1988Date of Patent: May 8, 1990Assignee: Bayer AktiengesellschaftInventors: Udo Eckstein, Hubertus Psaar
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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: 4886806Abstract: Falvone-3-carboxylic acid compounds corresponding to the Formula I: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 represent hydrogen, lower alkyl, halogen, hydroxy, or etherified or esterified hydroxy, and Z--R.sup.6 stands for a basically substituted alkoxy or amino group, as well as processes and intermediate products for their production. The compounds exhibit inflammation-inhibiting pharmacological activity.Type: GrantFiled: May 5, 1988Date of Patent: December 12, 1989Assignee: Kali-Chemie Pharma GmbHInventors: Rainer Walenta, Reiner Muller-Peddinghaus, Ivan Ban, Michael Wurl, Ulf Preuschoff
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Patent number: 4841050Abstract: Benzopyrans of the formula ##STR1## where X is a radical ##STR2## and R.sup.1, R.sup.2, R.sup.3, R.sup.4 and the ring A have the meanings stated in the description, a process for their preparation, and their use in pressure-sensitive or heat-sensitive layers.Type: GrantFiled: March 12, 1987Date of Patent: June 20, 1989Assignee: BASF AktiengesellschaftInventors: Andreas Guentner, Udo Mayer, Andreas Oberlinner
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Patent number: 4745114Abstract: The invention provides fungicidal compositions comprising as an active ingredient a compound having the general formula (I): ##STR1## or a stereoisomer thereof, wherein X is a methylene group and Y is an oxygen atom, or X is an oxygen atom and Y is a methylene or CHOH group; R.sup.1 and R.sup.2, which may be the same or different, are hydrogen or halogen atoms, or alkyl, alkenyl, alkynyl, alkoxy, haloalkyl, or haloalkoxy groups; R.sup.3 and R.sup.4, which may be the same or different, are alkyl groups containing from 1 to 8 carbon atoms, or --NR.sup.3 R.sup.4 is a 5- or 6-membered heterocyclic ring, optionally substituted by alkyl, aryl, aralkyl, hydroxy, alkoxy or aryloxy groups; or an acid addition salt of such a compound.Type: GrantFiled: June 2, 1986Date of Patent: May 17, 1988Assignee: Imperial Chemical Industries PLCInventors: Alison Elliott, Vivienne Anthony
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Patent number: 4722925Abstract: A class of bicyclic benzo-oxy heterocyclic ether and thioether compounds exhibiting pharmacological activity, including anti-secretory and anti-ulcerogenic activity, pharmaceutical compositions comprising these compounds, and methods for the treatment of gastro-intestinal hyperacidity and ulcerogenic disorders in mammals using said compositions.Type: GrantFiled: March 3, 1987Date of Patent: February 2, 1988Assignee: Rorer Pharmaceutical CorporationInventors: Donald E. Kuhla, Henry F. Campbell, William L. Studt, Kent W. Neuenschwander
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Patent number: 4665202Abstract: The invention relates to pharmaceutical preparations containing compounds of formula I ##STR1## in which X.sub.1 and X.sub.2, independently of each other, represent hydrogen, halogen, unsubstituted or substituted amino or a quaternary ammonium salt; etherified or esterified hydroxy; free, etherified, esterified or oxidized mercapto; nitro; functionally modified formyl; free or functionally modified carboxyl; acyl; an unsubstituted or substituted hydrocarbon radical, or an unsubstituted or substituted heterocyclic radical; with the proviso that at least one of the radicals X.sub.1 and X.sub.2 is bonded by a carbon atom to the ring system and with the proviso that X.sub.1 and X.sub.2 cannot be together halogen and formyl; in which Y represents oxygen, sulfur, sulfinyl or sulfonyl but must be sulfur, sulfinyl or sulfonyl, if X.sub.1 is hydrogen and X.sub.Type: GrantFiled: August 24, 1984Date of Patent: May 12, 1987Assignee: Zyma SAInventors: Christian G. Rimbault, Philippe M. Narbel
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Patent number: 4652649Abstract: A new class of anti-spasmodic compounds having two branch chains is provided. The compounds have the general formula: ##STR1## wherein the substituents are defined hereinbelow.Type: GrantFiled: February 20, 1985Date of Patent: March 24, 1987Assignee: United Pharmaceuticals, Inc.Inventor: William M. Davis
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Patent number: 4634768Abstract: This invention relates to derivatives of 3-methylflavone-8-carboxylic acid represented by the formula (1) ##STR1## wherein R represents a hydrogen atom, a lower alkyl group or a group ##STR2## (wherein R.sup.1 and R.sup.2 represent a lower alkyl group or R.sup.1 and R.sup.2, when taken together with the nitrogen atom to which they are attached, may form a heterocyclic ring with or without an intervening hetero atom, and n is an integer of 1 to 4), and X represents a halogen atom, which are useful as intermediates.This invention also relates to processes for preparing the same.Type: GrantFiled: April 4, 1985Date of Patent: January 6, 1987Assignees: Yamamoto Chemical Industrial Co., Ltd., Osaka Municipal GovernmentInventors: Hiroshige Inoue, Kenichi Fukushima, Ikuzo Nishiguchi
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Patent number: 4617414Abstract: A process for the preparation of phosphate compounds comprising (1) reacting an inorganic phosphate salt with epihalohydrin to obtain a phosphate ester and (2) reacting the phosphate ester with a substituted amine wherein step (1) is carried out at a pH of from about 5.4 to 7.0.Type: GrantFiled: September 10, 1984Date of Patent: October 14, 1986Assignee: Johnson & Johnson Baby Products CompanyInventors: Elvin R. Lukenbach, Richard R. Tenore
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Patent number: 4617314Abstract: Benzofuran- and benzopyran-carboxamide derivatives of the formula: ##STR1## wherein l is 1 or 2; X is hydrogen atom, amino group or halogen atom; Y is --S(O).sub.m --R.sup.3 wherein R.sup.3 is lower alkyl group and m is 0, 1 or 2, or ##STR2## wherein R.sup.4 and R.sup.5 are the same or different and are each hydrogen atom or lower alkyl group; R.sup.1 is hydrogen atom, lower alkyl group, arylthiomethyl group, halogenomethyl group or ##STR3## wherein R.sup.6 and R.sup.7 are the same or different and are each hydrogen atom or lower alkyl group or R.sup.6 and R.sup.7 together with the adjacent nitrogen atom form a hetrocycle; R.sup.2 is hydrogen atom or lower alkyl group; and Z is ##STR4## wherein p is 2 or 3, R.sup.8 and R.sup.9 are the same or different and are each lower alkyl group or R.sup.8 and R.sup.9 together with the adjacent nitrogen atom form a heterocycle, or ##STR5## wherein q is 0 or 1, n is 1 or 2, R.sup.Type: GrantFiled: March 20, 1984Date of Patent: October 14, 1986Assignee: Yoshitomi Pharmaceutical Industries Ltd.Inventors: Tetsuya Tahara, Kiyoharu Hayano, Michihide Setoguchi, Takemi Fukuda
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Patent number: 4605740Abstract: The present invention relates to a process for the production of N-substituted acrylic acid amides by conversion of 2-carboalkoxy-t-oxabicyclo(2,2,1)hept-5-enes with primary or secondary amines to 2-carboxamide-7-oxabicyclo(2,2,1)hept-5-enes and the thermal decomposition of the latter, preferably in the presence of Lewis acids and in a vacuum, to furane and N-substituted acrylic acid amides. The process according to the invention results in high purity N-substituted acrylic acid amides that are, in the main, free of bifunctional monomers which would disrupt the subsequent polymerization of the N-substituted acrylic acid amides by undesired cross-linking.Type: GrantFiled: September 22, 1983Date of Patent: August 12, 1986Assignee: Chemische Fabrik Stockhausen GmbHInventor: Alfons Landscheidt
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Patent number: 4602034Abstract: The invention concerns: (oxo-4-4H-(1)-benzopyran-8-yl) alkanoic acids and their derivatives, their manufacture, represented by the formula: ##STR1## where Ar is hydrogen, a phenyl radical which may or may not be substituted, thenyl, furyl, naphthyl, a lower alkyl, cycloalkyl, aralkyl radical; B is a linear or branched lower alkyl radical, either saturated or ethylinically unsaturated; R.sub.1 is hydrogen or a phenyl radical; X is hydrogen or a lower alkyl or alkoxy radical and n=1, as well as salts, esters, aminoesters and amides.Compounds and their derivatives may be used as medicines, in particular in the control of tumors.Type: GrantFiled: November 6, 1984Date of Patent: July 22, 1986Assignee: Lipha, Lyonnaise Industrielle PharmaceutiqueInventors: Philippe Briet, Jean-Jacques Berthelon, Francois Collonges
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Patent number: 4594345Abstract: 3-methylflavone derivatives which are useful in the treatment of allergies, asthma and inflammation.Type: GrantFiled: June 24, 1983Date of Patent: June 10, 1986Assignee: Nippon Shinyaku Co. Ltd.Inventors: Hiroshi Enomoto, Tadatoshi Nomura, Yoshiaki Aoyagi, Shoichi Chokai, Masao Murase, Kichiro Inoue, Ichiro Shirahase
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Patent number: 4577021Abstract: 1H-2-benzopyran-1-yl alkyl or 1-(isochroman-1-yl) alkyl 4-phenyl piperazines are prepared and exhibit antipsychotic and hypotensive activity.Type: GrantFiled: April 1, 1985Date of Patent: March 18, 1986Assignee: The Upjohn CompanyInventor: John M. McCall
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Patent number: 4548929Abstract: Novel heterobicyclic compounds of Formula I, processes for preparing same and pesticidal compositions and methods are described.Type: GrantFiled: April 18, 1983Date of Patent: October 22, 1985Assignee: SDS Biotech CorporationInventors: Thomas A. Magee, Robert D. Battershell, Lawrence E. Limpel, Andrew W. Ho, Arthur W. Friedman, H. Glenn Corkins, William W. Brand, Russell Buchman, Louis Storace, Edmond R. Osgood
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Patent number: 4525356Abstract: Derivatives of N-substituted flavone-8-carboxamides represented by general formula (I) ##STR1## wherein R.sub.1 represents a hydrogen atom, a methyl group or an ethyl group, R.sub.2 represents a hydrogen atom, a lower alkyl group, a lower alkoxyl group, a halogen atom or a nitro group, R.sub.3 represents a hydrogen atom or a lower alkyl group, k represents 0, 1, 2, or 3, m represents 0 or 1; X and Y, which must be different, represent a hydrogen atom or methyl group. A represents an amino group having the formula ##STR2## wherein, R.sub.4 and R.sub.5, which may be the same or different, represent a lower alkyl group or a cyclic amino group together with the nitrogen atom and with or without an oxygen atom, R.sub.6 represents a lower alkyl group and n represents 2 or 3, are disclosed, as well as pharmaceutical compositions thereof and method of treating therewith.The N-substituted flavone-8-carboxamides derivatives are useful as agents for treatment of dysurea.Type: GrantFiled: October 28, 1983Date of Patent: June 25, 1985Assignee: Hokuriku Pharmaceutical Co., Ltd.Inventors: Yasuo Itho, Hideo Kato, Nobuo Ogawa, Kagari Yamagishi, Eiichi Koshinaka, Kazuya Mitani
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Patent number: 4496565Abstract: Compounds of formula (I): ##STR1## a pharmaceutically acceptable salt or solvate thereof having anti-hypertensive activity, a process for their preparation and their use as pharmaceuticals.Type: GrantFiled: October 17, 1983Date of Patent: January 29, 1985Assignee: Beecham Group p.l.c.Inventors: John M. Evans, Valerie A. Ashwood
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Patent number: 4487774Abstract: Amino derivatives of isochromans are described. These compounds exhibit antipsychotic and hypotensive activity.Type: GrantFiled: April 21, 1982Date of Patent: December 11, 1984Assignee: The Upjohn CompanyInventor: John M. McCall
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Patent number: 4486428Abstract: Bicyclic fused benzenoid compounds of the formula ##STR1## and pharmaceutically acceptable cationic and acid addition salts thereof, where M is O, CH.sub.2 or NR.sub.6 ; R.sub.6 is hydrogen, formyl, carbobenzyloxy or certain carboalkoxyalkyl, alkanoyl, alkyl, aralkyl or aralkylcarbonyl groups;A' is:(1) A where one of A and B is hydrogen such that when A is hydrogen, B is C(R.sub.2 R.sub.3)(CH.sub.2).sub.f Q and f is 1 or 2; when B is hydrogen, A is C(R.sub.2 R.sub.3)(CH.sub.2).sub.f Q and f is 0 or 1, when taken together A and OR.sub.1 form a lactone or certain derivatives thereof;(2) A' is ##STR2## (3) A' is Q.sub.3 ; Q is CO.sub.2 R.sub.7, COR.sub.8, C(OH)R.sub.8 R.sub.9, CN, CONR.sub.12 R.sub.13, CH.sub.2 NR.sub.12 R.sub.13, CH.sub.2 NHCOR.sub.14, CH.sub.2 NHSO.sub.2 R.sub.17 or 5-tetrazoyl;Q.sub.3 is ##STR3## 5-tetrazolyl, CH.sub.2 CONHCOR.sub.7, COOH or certain ester, amide, carboximido or sulfonimido derivatives thereof, CONHOH, CONHCONH.sub.2, or COCH.sub.2 Q.sub.4 where Q.sub.Type: GrantFiled: January 13, 1983Date of Patent: December 4, 1984Assignee: Pfizer Inc.Inventors: James F. Eggler, Michael R. Johnson, Lawrence S. Melvin, Jr.
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Patent number: 4452811Abstract: A selective process is described for producing monohalogenated derivatives of 7-hydroxy coumarin wherein the halo substituent is at the desired position and the final product is free of other monohalogenated isomers. The resulting products and pharmaceutical compositions containing the same, especially those wherein the halo substituent is at the 8 position, have valuable specific coronary vasodilating activity.Type: GrantFiled: February 1, 1982Date of Patent: June 5, 1984Assignee: Fidia S.p.A.Inventor: Francesco della Valle
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Patent number: 4447622Abstract: The laevo and dextro forms of dl-3,4-trans-2,2-disubstituted-3,4-diarylchromans and similar derivatives thereof have substantially double the post-coital anti-fertility activity of the known racemic compound. The resolution of such known compound into the l- and d-isomeric forms may be carried out using di-p-toluoyl-l-tartaric acid monohydrate or di-p-toluoyl-d-tartaric acid.Type: GrantFiled: September 22, 1981Date of Patent: May 8, 1984Assignee: Council of Scientific and Industrial Research Rafi MargInventors: Mohammad Salman, Suprabhat Ray, Ved P. Kamboj, Nitya Anand
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Patent number: 4382036Abstract: Novel amphoteric and zwitterionic betaine compounds containing at least one anion having a phosphorus-oxygen-phosphorus bond and processes for their preparation are described.Type: GrantFiled: May 15, 1981Date of Patent: May 3, 1983Assignee: Johnson & Johnson Baby Products CompanyInventors: Martin K. O. Lindemann, Elvin R. Lukenbach, Robert J. Verdicchio
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Patent number: 4366163Abstract: Compounds of the formula (I) ##STR1## and salts and pro-drugs thereof, wherein: R.sub.1 is a hydrogen atom or a lower alkyl group;R.sub.2 is a hydrogen atom or a lower alkyl group;R.sub.3 is a hydrogen atom or a lower alkyl group;R.sub.4 is a hydrogen atom or an alkyl group;R.sub.5 is a lower alkyl or a substituted alkyl group;or R.sub.4 and R.sub.5 are joined so that together with the nitrogen atom to which they are attached they form a 5-, 6- or 7-membered ring optionally containing an oxygen or sulphur atom;R.sub.6 is an electron donating group;R.sub.7 is an electron withdrawing group; andthe NR.sub.4 R.sub.5 and OR.sub.3 moieties are trans having compositions containing them and processes for their preparation.Type: GrantFiled: September 12, 1980Date of Patent: December 28, 1982Assignee: Beecham Group LimitedInventors: John M. Evans, Graham A. Showell, Charles S. Fake
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Patent number: 4364942Abstract: This invention relates to a novel series of 2,3-dihydro-imidazo[2,1-b]benzothiazoles which display monoamine oxidase inhibiting activities.Type: GrantFiled: March 30, 1981Date of Patent: December 21, 1982Assignee: Janssen Pharmaceutica N.V.Inventor: Victor Sipido
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Patent number: 4363811Abstract: Compounds of the formula (I): ##STR1## and salts and pro-drugs thereof, wherein: R.sub.1 is a hydrogen atom or a lower alkyl group;R.sub.2 is a hydrogen atom or a lower alkyl group;R.sub.3 is a hydrogen atom or a lower alkyl group;R.sub.4 is a hydrogen atom or an alkyl group;R.sub.5 is a lower alkyl or a substituted alkyl group;or R.sub.4 and R.sub.5 are joined so that together with the nitrogen atom to which they are attached they form a 5-, 6- or 7-membered ring optionally containing an oxygen or sulphur atom;R.sub.6 is an electron donating group;R.sub.7 is an electron withdrawing group; andthe NR.sub.4 R.sub.5 and OR.sub.3 moieties are trans having antihypertensive activity, pharmaceutical compositions containing them and processes for their preparation.Type: GrantFiled: September 12, 1980Date of Patent: December 14, 1982Assignee: Beecham Group LimitedInventors: John M. Evans, Graham A. Showell, Charles S. Fake
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Patent number: 4337338Abstract: The present invention provides 2,5-inter-o-phenylene-3,4-dinor-5,9.alpha.-epoxy-6-iodo-PGF.sub.1 amides. These compounds are intermediates for preparing 2,5-inter-o-phenylene-3,4-dinor-prostacyclin analogs, which are useful for pharmacological purposes, e.g., as antithrombotic agents.Type: GrantFiled: July 3, 1980Date of Patent: June 29, 1982Assignee: The Upjohn CompanyInventors: Udo F. Axen, John C. Sih
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Patent number: 4337203Abstract: The present invention provides 2,5-inter-o-phenylene-3,4-dinor-5,9.alpha.-epoxy-PGF.sub.1 amides. These compounds are useful for a wide variety of pharmacological and therapeutical purposes, e.g., as antithrombotic agents.Type: GrantFiled: July 3, 1980Date of Patent: June 29, 1982Assignee: The Upjohn CompanyInventors: Udo F. Axen, John C. Sih
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Patent number: 4334067Abstract: A flavan compound represented by the formula (I) ##STR1## wherein R, R.sub.1, R.sub.2 and R.sub.3 are as defined above, and the pharmaceutically acceptable acid addition salt thereof, which are useful as pharmaceutical agent having anti-convulsive, anti-ulcer, anti-arrythmic and diuretic activities.Type: GrantFiled: October 29, 1980Date of Patent: June 8, 1982Assignee: Maruko Seiyaku Co., Ltd.Inventors: Sachio Ohno, Mitsuaki Nagasaka, Kazuo Kato
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Patent number: 4312810Abstract: This invention relates to certain structural and pharmacological analogs of prostacyclin (PGI.sub.2) and 5,6-dehydroprostacyclin (PGI.sub.1) and 5,9.alpha.-epoxy-9-deoxy-PGF.sub.1, wherein between the position beta to the carboxy (C-2) and C-5 there is substituted an inter-o-phenylene for the ethylene chain. These novel 2,5-inter-o-phenylene-3,4-dinor-prostaglandin or prostacyclin-type compounds are useful for certain of the same pharmacological purposes as prostacyclin, particularly being smooth muscle stimulators, blood pressure depressors and platelet aggregation inhibitors. Also provided are novel intermediates therefor, namely corresponding interphenylene-containing PGF.sub.2.alpha. and 5-halo-PGI.sub.1 and 6-halo-5,9.alpha.-epoxy-9-deoxy-PGF.sub.1 compounds.Type: GrantFiled: July 31, 1979Date of Patent: January 26, 1982Assignee: The Upjohn CompanyInventors: Udo F. Axen, John C. Sih
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Patent number: 4303656Abstract: A compound of the general formula (III), having anorexic activity: ##STR1## or a salt thereof, wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 may be the same or different and are each a hydrogen or halogen atom, or a trifluoromethyl, C.sub.1 to C.sub.4 alkyl, C.sub.1 to C.sub.4 alkoxy, hydroxyl, carboxyl, C.sub.1 to C.sub.4 alkoxycarbonyl, amino or acetamido group; R.sub.6 is a hydrogen atom or a C.sub.1 to C.sub.4 alkyl group; X is a straight or branched alkylene group of up to 4 carbon atoms; and R.sub.7 and R.sub.8 which may be the same or different are each a hydrogen atom or a C.sub.1 to C.sub.4 alkyl group, or R.sub.7 is joined to R.sub.8 so that NR.sub.7 R.sub.8 forms a 5-7 membered heterocyclic ring.Type: GrantFiled: May 1, 1980Date of Patent: December 1, 1981Assignee: Beecham Group LimitedInventors: John T. Sime, Anthony T. Ainsworth
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Patent number: 4299959Abstract: A fluorescent pigment consisting of N-substituted iminocoumarins of the general formula I, ##STR1## wherein X.sub.1 is a cyano group, a carboxamido group or an aryl or a heteroaryl radical linked directly or through a --CO or --SO.sub.2 group,X.sub.2 is an amino group, hydroxy group or an alkoxy group and when it is an amino group, may carry an optionally substituted alkylene or alkylidene group bound in ortho position to the nitrogen atom and in para position with respect to the coumarin oxygen atom,X.sub.3 is a hydrogen atom, a halogen atom or a cyano group andX.sub.4 is a functionally converted carboxyl groups. The new dyestuffs dye polyester fiber in orange or red shades with good fastness.Type: GrantFiled: January 31, 1979Date of Patent: November 10, 1981Assignee: Ciba-Geigy CorporationInventor: Nalin B. Desai
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Patent number: 4296039Abstract: A selective process is described for producing monohalogenated derivatives of 7-hydroxy coumarin wherein the halo substituent is at the desired position and the final product is free of other monohalogenated isomers. The resulting products, especially those wherein the halo substituent is at the 8 position, have valuable specific coronary vasodilating activity.Type: GrantFiled: January 15, 1980Date of Patent: October 20, 1981Assignee: Fidia S.p.A.Inventor: Francesco Della Valle
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Patent number: 4251537Abstract: Amino chromanols, their preparation and anti-hypertensive compositions containing the compounds in hypotensive amounts with a pharmaceutically acceptable carrier for oral or parenteral administration. Pharmaceutically acceptable salts and O-acyl, particularly O-acetyl, derivatives are described. The compounds exist as racemates and optically active isomers.Type: GrantFiled: December 18, 1978Date of Patent: February 17, 1981Assignee: Beecham Group LimitedInventor: John M. Evans
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Patent number: 4234726Abstract: Compounds of the formula (I): ##STR1## or a pharmaceutically acceptable salt thereof wherein the NR.sub.1 R.sub.2 moiety is a 5-, 6-, or 7-membered saturated heterocyclic ring; R.sub.3 is hydrogen, alkyl of 1 to 4 carbon atoms or acyl of 1 to 4 carbon atoms; R.sub.4 is naphthyl or phenyl unsubstituted or substituted by one or two substituents selected from the group consisting of fluorine, chlorine, bromine, methoxyl, benzyloxyl, trifluoromethyl, methyl, cyano, nitro, acetoxyl, amino, methylamino, ethylamino, dimethylamino, diethylamino, acetamide, hydroxyl, methoxycarbonyl, ethoxycarbonyl, carboxamido, sulphonamido, carboxy, trifluoromethylthio, trifluoromethoxyl, methylsulphonyl, trifluomethylsulphonyl and methylthio; R.sub.5 is hydrogen or alkyl of 1 to 4 carbon atoms; R.sub.6 is hydrogen or alkyl of 1 to 4 carbon atoms; X is oxygen and the dotted line represents a single or double bond.Type: GrantFiled: May 9, 1979Date of Patent: November 18, 1980Assignee: Beecham Group LimitedInventor: Derek V. Gardner
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Patent number: 4230850Abstract: Novel 3-substituted-4-aminoalkoxy-5,6-condensed ring-2-pyranones are disclosed as having utility as pharmacologically active compounds, in particular vasodilatory, hypotensive, anti-ischemic and anti-tussive activity. The compounds may be 3-phenyl-4-morpholinoalkoxy-coumarins. Administration may be by the oral or parenteral route. Intermediates useful in the production of these compounds are also disclosed.Type: GrantFiled: March 9, 1979Date of Patent: October 28, 1980Assignee: LIPHA, Lyonnaise Industrielle PharmaceutiqueInventors: Philippe Briet, Jean-Jacques Berthelon, Jean-Claude Depin
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Patent number: 4220645Abstract: A chromone derivative has the formula: ##STR1## in which one of the radicals R, R' is a hydrogen atom or a lower alkyl radical and the other of the radicals is an aminoalkyl oxy benzoyl group having the formula: ##STR2## The derivative can be of use in the pharmaceutical industry in drugs for treating heart disorders.Type: GrantFiled: December 29, 1977Date of Patent: September 2, 1980Assignee: Thea (Therapeutique et Applications) SAInventor: Henri Chibret
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Patent number: 4205082Abstract: New benzopyrane derivatives of the general formula ##STR1## in which R is free, esterified or amidated carboxyl, Ph is 1,2-phenylene which contains the group R--CO--NR.sub.3 -- and is otherwise unsubstituted or is substituted, X is a group of the formula --CO--CR.sub.1 .dbd.CR.sub.2 --, in which R.sub.1 and R.sub.2 independently of one another are hydrogen, acyl or a substituted or unsubstituted hydrocarbon radical or a hetero-analogue thereof, or conjointly are 3-membered to 5-membered lower alkylene, and R.sub.2 can also be free or etherified hydroxyl or hydroxyl etherified by an organic carboxylic acid, and R.sub.3 is hydrogen or lower alkyl, are useful as anti-allergic agents.Type: GrantFiled: August 19, 1977Date of Patent: May 27, 1980Assignee: Ciba-Geigy CorporationInventor: Pier G. Ferrini
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Patent number: 4187233Abstract: A pressure- or heat-sensitive recording material which contains as color former at least one 2,2-diarylchromeno compound of the formula ##STR1## wherein V.sub.1 and V.sub.2, each independently of the other, represent hydrogen, halogen, lower alkyl or lower alkoxy,Y.sub.1 and Y.sub.2, each independently of the other, represent hydrogen, --O--R.sub.1 or ##STR2## X.sub.1 and X.sub.2, each independently of the other, represent hydrogen, alkyl of up to 12 carbon atoms which is unsubstituted or substituted by halogen, or represent benzyl, phenyl, or benzyl or phenyl which is substituted by halogen, nitro, lower alkyl, lower alkoxy or the amino group ##STR3## and the ring A is unsubstituted or substituted by halogen, nitro, lower alkyl, --O--R.sub.5 or ##STR4## or contains a fused benzene ring, and R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.Type: GrantFiled: January 30, 1978Date of Patent: February 5, 1980Assignee: Ciba-Geigy CorporationInventor: Jean C. Petitpierre
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Patent number: 4183946Abstract: Substituted 2-vinyl chromones are disclosed, wherein the chromone ring has an alkyl or alkenyl substituent at the 3-position, and a styryl substituent at the 2-position. The compounds exhibit anti-allergy activity and can be used to treat allergic conditions.Type: GrantFiled: July 24, 1978Date of Patent: January 15, 1980Assignee: Carlo Erba S.p.A.Inventors: Gianfederico Doria, Ciriaco Romeo, Francesco Lauria, Maria L. Corno, Piernicola Giraldi, Marcello Tibolla
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Patent number: 4181665Abstract: Isochromans, isothiochromans, 2-benzoxepins, and 2-benzothiepins are described. These compounds are useful for preparing corresponding amino derivatives that possess antihypertensive and CNS activity.Type: GrantFiled: January 2, 1979Date of Patent: January 1, 1980Assignee: The Upjohn CompanyInventor: John M. McCall
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Patent number: 4170703Abstract: The present invention provides 5-hydroxy-PGI.sub.1, morpholinylamides, which are useful pharmacological agents. These analogs of prostaglandin I.sub.1 are useful for the stimulation of mammalian smooth muscle tissues.Type: GrantFiled: April 24, 1978Date of Patent: October 9, 1979Assignee: The Upjohn CompanyInventors: Roy A. Johnson, John C. Sih
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Patent number: 4166062Abstract: 1-Alkoxyethanol-isochromas, -isothiochromas, -2-benzoxepins, and -2-benzothiepins are described. These compounds are useful for preparing the corresponding aminoalkoxyalkyl derivatives that possess antihypertensive and CNS activity.Type: GrantFiled: July 21, 1978Date of Patent: August 28, 1979Assignee: The Upjohn CompanyInventors: John M. McCall, Ruth E. TenBrink
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Patent number: 4160028Abstract: Substituted 2-cyclopropylchromones, process of preparation, pharmaceutical compositions and method of treating allergies are disclosed.Type: GrantFiled: July 3, 1978Date of Patent: July 3, 1979Assignee: Carlo Erba S.p.A.Inventors: Gianfederico Doria, Ciriaco Romeo, Maria L. Corno, Francesco Lauria, Piero Sberze, Marcellino Tibolla
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Patent number: 4153618Abstract: A fluorescent pigment consisting of N-substituted iminocoumarins of the general formula I, ##STR1## wherein X.sub.1 is a cyano group, a carboxamido group or an aryl or a heteroaryl radical linked directly or through a --CO or --SO.sub.2 group,X.sub.2 is an amino group, hydroxy group or an alkoxy group and when it is an amino group, may carry an optionally substituted alkylene or alkylidene group bound in ortho position to the nitrogen atom and in para position with respect to the coumarin oxygen atom,X.sub.3 is a hydrogen atom, a halogen atom or a cyano group andX.sub.4 is a functionally converted carboxyl groups. The new dyestuffs dye polyester fiber in orange or red shades with good fastness.Type: GrantFiled: April 4, 1977Date of Patent: May 8, 1979Assignee: Ciba-Geigy CorporationInventor: Nalin B. Desai
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Patent number: 4151291Abstract: The invention provides novel esters of 7-hydroxycoumarin of the formula ##STR1## in which each of R.sub.1 and R.sub.2 represents a hydrogen atom, a C.sub.1 -C.sub.4 alkyl, C.sub.2 -C.sub.4 alkenyl, carboxy, carboxylate, C.sub.2 -C.sub.5 alkoxycarbonyl or nitrophenyl group, and R.sub.3 represents a hydrogen atom or a group of the formula --CH.sub.2 --Z in which Z represents a di(C.sub.1 -C.sub.4 alkyl)amino group, or a saturated heterocyclic amino radical containing 5 to 7 ring members which may contain a further heteroatom, and their pharmaceutically acceptable acid addition salts. The compounds are useful as medicaments, in particular as analgesics.Type: GrantFiled: November 17, 1977Date of Patent: April 24, 1979Assignee: UniclerInventor: Francois M. J. Vallet
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Patent number: 4148900Abstract: Chromone compounds carrying a pyridyl substituent at the 2-position are disclosed, such as, for instance, 6-carboxy-2-(2'-pyridyl)-chromone. The disclosed compounds are useful in the treatment of allergies.Type: GrantFiled: September 16, 1977Date of Patent: April 10, 1979Assignee: Carlo Erba S.p.A.Inventors: Gianfederico Doria, Piernicola Giraldi, Francesco Lauria, Maria L. Corno, Piero Sberze, Marcello Tibolla
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Patent number: 4144336Abstract: Novel 2-benzopyranone compounds of the formula ##STR1## wherein X is a 3,4,5-trimethoxybenzoyl group or a 3,4,5-trimethoxycinnamoyl group; and eachR individually is selected from the group consisting of alkylamino and dialkylamino in which one carbon atom in the alkyl moiety may be replaced by an oxygen atom and one hydrogen atom may be replaced by a hydroxyl group which may in turn be esterified with a 3,4,5-trimethoxybenzoyl or 3,4,5-trimethoxycinnamoyl group; amino substituted once or twice by alkenyl, aralkyl, or cycloalkyl; or a 4- to 7-membered N-containing heterocyclic ring linked through a nitrogen atom and which contains up to 3 hetero atoms, which heterocyclic ring may be substituted by phenyl, alkyl or hydroxyalkyl, wherein the hydroxy group may be esterified by a 3,4,5-trimethoxy benzoyl or 3,4,5-trimethoxy cinnamoyl group;Or a salt of each compound with a physiologically acceptable acid; possess outstanding activity as coronary dilators. Processes for producing such compounds are also disclosed.Type: GrantFiled: July 8, 1976Date of Patent: March 13, 1979Assignee: Troponwerke Dinklage & Co.Inventors: Karl-Heinz Boltze, Peter-Rudolf Seidel, Haireddin Jacobi, Helmut Schwarz
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Patent number: 4133880Abstract: N.sup.2 -substituted-L-arginine esters and amides, and the pharmaceutically acceptable acid addition salts thereof have been found to be effective as pharmaceutical agents for the inhibition and suppression of thrombosis.Type: GrantFiled: July 28, 1977Date of Patent: January 9, 1979Assignees: Mitsubishi Chemical Industries Ltd., Shosuke OkamotoInventors: Shosuke Okamoto, Akiko Hijikata, Ryoji Kikumoto, Yoshikuni Tamao, Kazuo Ohkubo, Tohru Tezuka, Shinji Tonomura
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Patent number: RE30739Abstract: Compounds within formula ##STR1## and their salts wherein X is alkylene of 2-4 carbon atoms; R.sub.1 is hydrogen or alkyl of 1-6 carbon atoms; R.sub.2 is hydrogen, alkyl of 1-6 carbon atoms or benzyl, or R.sub.1 and R.sub.2 together with the nitrogen atom to which they are attached form a 5-, 6- or 7-membered saturated ring; R.sub.3 is aryl; R.sub.4 is hydrogen or alkyl of 1-4 carbon atoms; and R.sub.5 is hydrogen or alkyl of 1-4 carbon atoms; have been found to possess mood-modifying and anorexia inducing activity.Type: GrantFiled: May 14, 1979Date of Patent: September 8, 1981Assignee: Beecham Group LimitedInventor: Derek V. Gardner