The Additional Six-membered Hetero Ring Is One Of The Cyclos In A Bicyclo Ring System Patents (Class 544/151)
  • Patent number: 4923641
    Abstract: 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: Grant
    Filed: September 20, 1988
    Date of Patent: May 8, 1990
    Assignee: Bayer Aktiengesellschaft
    Inventors: Udo Eckstein, Hubertus Psaar
  • Patent number: 4914206
    Abstract: 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: Grant
    Filed: December 15, 1988
    Date of Patent: April 3, 1990
    Assignee: Takeda Chemical Industries, LTD.
    Inventors: Isao Minamida, Naoto Hashimoto
  • Patent number: 4886806
    Abstract: 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: Grant
    Filed: May 5, 1988
    Date of Patent: December 12, 1989
    Assignee: Kali-Chemie Pharma GmbH
    Inventors: Rainer Walenta, Reiner Muller-Peddinghaus, Ivan Ban, Michael Wurl, Ulf Preuschoff
  • Patent number: 4841050
    Abstract: 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: Grant
    Filed: March 12, 1987
    Date of Patent: June 20, 1989
    Assignee: BASF Aktiengesellschaft
    Inventors: Andreas Guentner, Udo Mayer, Andreas Oberlinner
  • Patent number: 4745114
    Abstract: 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: Grant
    Filed: June 2, 1986
    Date of Patent: May 17, 1988
    Assignee: Imperial Chemical Industries PLC
    Inventors: Alison Elliott, Vivienne Anthony
  • Patent number: 4722925
    Abstract: 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: Grant
    Filed: March 3, 1987
    Date of Patent: February 2, 1988
    Assignee: Rorer Pharmaceutical Corporation
    Inventors: Donald E. Kuhla, Henry F. Campbell, William L. Studt, Kent W. Neuenschwander
  • Patent number: 4665202
    Abstract: 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: Grant
    Filed: August 24, 1984
    Date of Patent: May 12, 1987
    Assignee: Zyma SA
    Inventors: Christian G. Rimbault, Philippe M. Narbel
  • Patent number: 4652649
    Abstract: 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: Grant
    Filed: February 20, 1985
    Date of Patent: March 24, 1987
    Assignee: United Pharmaceuticals, Inc.
    Inventor: William M. Davis
  • Patent number: 4634768
    Abstract: 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: Grant
    Filed: April 4, 1985
    Date of Patent: January 6, 1987
    Assignees: Yamamoto Chemical Industrial Co., Ltd., Osaka Municipal Government
    Inventors: Hiroshige Inoue, Kenichi Fukushima, Ikuzo Nishiguchi
  • Patent number: 4617414
    Abstract: 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: Grant
    Filed: September 10, 1984
    Date of Patent: October 14, 1986
    Assignee: Johnson & Johnson Baby Products Company
    Inventors: Elvin R. Lukenbach, Richard R. Tenore
  • Patent number: 4617314
    Abstract: 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: Grant
    Filed: March 20, 1984
    Date of Patent: October 14, 1986
    Assignee: Yoshitomi Pharmaceutical Industries Ltd.
    Inventors: Tetsuya Tahara, Kiyoharu Hayano, Michihide Setoguchi, Takemi Fukuda
  • Patent number: 4605740
    Abstract: 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: Grant
    Filed: September 22, 1983
    Date of Patent: August 12, 1986
    Assignee: Chemische Fabrik Stockhausen GmbH
    Inventor: Alfons Landscheidt
  • Patent number: 4602034
    Abstract: 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: Grant
    Filed: November 6, 1984
    Date of Patent: July 22, 1986
    Assignee: Lipha, Lyonnaise Industrielle Pharmaceutique
    Inventors: Philippe Briet, Jean-Jacques Berthelon, Francois Collonges
  • Patent number: 4594345
    Abstract: 3-methylflavone derivatives which are useful in the treatment of allergies, asthma and inflammation.
    Type: Grant
    Filed: June 24, 1983
    Date of Patent: June 10, 1986
    Assignee: Nippon Shinyaku Co. Ltd.
    Inventors: Hiroshi Enomoto, Tadatoshi Nomura, Yoshiaki Aoyagi, Shoichi Chokai, Masao Murase, Kichiro Inoue, Ichiro Shirahase
  • Patent number: 4577021
    Abstract: 1H-2-benzopyran-1-yl alkyl or 1-(isochroman-1-yl) alkyl 4-phenyl piperazines are prepared and exhibit antipsychotic and hypotensive activity.
    Type: Grant
    Filed: April 1, 1985
    Date of Patent: March 18, 1986
    Assignee: The Upjohn Company
    Inventor: John M. McCall
  • Patent number: 4548929
    Abstract: Novel heterobicyclic compounds of Formula I, processes for preparing same and pesticidal compositions and methods are described.
    Type: Grant
    Filed: April 18, 1983
    Date of Patent: October 22, 1985
    Assignee: SDS Biotech Corporation
    Inventors: 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
  • Patent number: 4525356
    Abstract: 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: Grant
    Filed: October 28, 1983
    Date of Patent: June 25, 1985
    Assignee: Hokuriku Pharmaceutical Co., Ltd.
    Inventors: Yasuo Itho, Hideo Kato, Nobuo Ogawa, Kagari Yamagishi, Eiichi Koshinaka, Kazuya Mitani
  • Patent number: 4496565
    Abstract: 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: Grant
    Filed: October 17, 1983
    Date of Patent: January 29, 1985
    Assignee: Beecham Group p.l.c.
    Inventors: John M. Evans, Valerie A. Ashwood
  • Patent number: 4487774
    Abstract: Amino derivatives of isochromans are described. These compounds exhibit antipsychotic and hypotensive activity.
    Type: Grant
    Filed: April 21, 1982
    Date of Patent: December 11, 1984
    Assignee: The Upjohn Company
    Inventor: John M. McCall
  • Patent number: 4486428
    Abstract: 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: Grant
    Filed: January 13, 1983
    Date of Patent: December 4, 1984
    Assignee: Pfizer Inc.
    Inventors: James F. Eggler, Michael R. Johnson, Lawrence S. Melvin, Jr.
  • Patent number: 4452811
    Abstract: 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: Grant
    Filed: February 1, 1982
    Date of Patent: June 5, 1984
    Assignee: Fidia S.p.A.
    Inventor: Francesco della Valle
  • Patent number: 4447622
    Abstract: 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: Grant
    Filed: September 22, 1981
    Date of Patent: May 8, 1984
    Assignee: Council of Scientific and Industrial Research Rafi Marg
    Inventors: Mohammad Salman, Suprabhat Ray, Ved P. Kamboj, Nitya Anand
  • Patent number: 4382036
    Abstract: 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: Grant
    Filed: May 15, 1981
    Date of Patent: May 3, 1983
    Assignee: Johnson & Johnson Baby Products Company
    Inventors: Martin K. O. Lindemann, Elvin R. Lukenbach, Robert J. Verdicchio
  • Patent number: 4366163
    Abstract: 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: Grant
    Filed: September 12, 1980
    Date of Patent: December 28, 1982
    Assignee: Beecham Group Limited
    Inventors: John M. Evans, Graham A. Showell, Charles S. Fake
  • Patent number: 4364942
    Abstract: This invention relates to a novel series of 2,3-dihydro-imidazo[2,1-b]benzothiazoles which display monoamine oxidase inhibiting activities.
    Type: Grant
    Filed: March 30, 1981
    Date of Patent: December 21, 1982
    Assignee: Janssen Pharmaceutica N.V.
    Inventor: Victor Sipido
  • Patent number: 4363811
    Abstract: 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: Grant
    Filed: September 12, 1980
    Date of Patent: December 14, 1982
    Assignee: Beecham Group Limited
    Inventors: John M. Evans, Graham A. Showell, Charles S. Fake
  • Patent number: 4337338
    Abstract: 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: Grant
    Filed: July 3, 1980
    Date of Patent: June 29, 1982
    Assignee: The Upjohn Company
    Inventors: Udo F. Axen, John C. Sih
  • Patent number: 4337203
    Abstract: 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: Grant
    Filed: July 3, 1980
    Date of Patent: June 29, 1982
    Assignee: The Upjohn Company
    Inventors: Udo F. Axen, John C. Sih
  • Patent number: 4334067
    Abstract: 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: Grant
    Filed: October 29, 1980
    Date of Patent: June 8, 1982
    Assignee: Maruko Seiyaku Co., Ltd.
    Inventors: Sachio Ohno, Mitsuaki Nagasaka, Kazuo Kato
  • Patent number: 4312810
    Abstract: 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: Grant
    Filed: July 31, 1979
    Date of Patent: January 26, 1982
    Assignee: The Upjohn Company
    Inventors: Udo F. Axen, John C. Sih
  • Patent number: 4303656
    Abstract: 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: Grant
    Filed: May 1, 1980
    Date of Patent: December 1, 1981
    Assignee: Beecham Group Limited
    Inventors: John T. Sime, Anthony T. Ainsworth
  • Patent number: 4299959
    Abstract: 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: Grant
    Filed: January 31, 1979
    Date of Patent: November 10, 1981
    Assignee: Ciba-Geigy Corporation
    Inventor: Nalin B. Desai
  • Patent number: 4296039
    Abstract: 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: Grant
    Filed: January 15, 1980
    Date of Patent: October 20, 1981
    Assignee: Fidia S.p.A.
    Inventor: Francesco Della Valle
  • Patent number: 4251537
    Abstract: 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: Grant
    Filed: December 18, 1978
    Date of Patent: February 17, 1981
    Assignee: Beecham Group Limited
    Inventor: John M. Evans
  • Patent number: 4234726
    Abstract: 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: Grant
    Filed: May 9, 1979
    Date of Patent: November 18, 1980
    Assignee: Beecham Group Limited
    Inventor: Derek V. Gardner
  • Patent number: 4230850
    Abstract: 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: Grant
    Filed: March 9, 1979
    Date of Patent: October 28, 1980
    Assignee: LIPHA, Lyonnaise Industrielle Pharmaceutique
    Inventors: Philippe Briet, Jean-Jacques Berthelon, Jean-Claude Depin
  • Patent number: 4220645
    Abstract: 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: Grant
    Filed: December 29, 1977
    Date of Patent: September 2, 1980
    Assignee: Thea (Therapeutique et Applications) SA
    Inventor: Henri Chibret
  • Patent number: 4205082
    Abstract: 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: Grant
    Filed: August 19, 1977
    Date of Patent: May 27, 1980
    Assignee: Ciba-Geigy Corporation
    Inventor: Pier G. Ferrini
  • Patent number: 4187233
    Abstract: 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: Grant
    Filed: January 30, 1978
    Date of Patent: February 5, 1980
    Assignee: Ciba-Geigy Corporation
    Inventor: Jean C. Petitpierre
  • Patent number: 4183946
    Abstract: 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: Grant
    Filed: July 24, 1978
    Date of Patent: January 15, 1980
    Assignee: Carlo Erba S.p.A.
    Inventors: Gianfederico Doria, Ciriaco Romeo, Francesco Lauria, Maria L. Corno, Piernicola Giraldi, Marcello Tibolla
  • Patent number: 4181665
    Abstract: 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: Grant
    Filed: January 2, 1979
    Date of Patent: January 1, 1980
    Assignee: The Upjohn Company
    Inventor: John M. McCall
  • Patent number: 4170703
    Abstract: 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: Grant
    Filed: April 24, 1978
    Date of Patent: October 9, 1979
    Assignee: The Upjohn Company
    Inventors: Roy A. Johnson, John C. Sih
  • Patent number: 4166062
    Abstract: 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: Grant
    Filed: July 21, 1978
    Date of Patent: August 28, 1979
    Assignee: The Upjohn Company
    Inventors: John M. McCall, Ruth E. TenBrink
  • Patent number: 4160028
    Abstract: Substituted 2-cyclopropylchromones, process of preparation, pharmaceutical compositions and method of treating allergies are disclosed.
    Type: Grant
    Filed: July 3, 1978
    Date of Patent: July 3, 1979
    Assignee: Carlo Erba S.p.A.
    Inventors: Gianfederico Doria, Ciriaco Romeo, Maria L. Corno, Francesco Lauria, Piero Sberze, Marcellino Tibolla
  • Patent number: 4153618
    Abstract: 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: Grant
    Filed: April 4, 1977
    Date of Patent: May 8, 1979
    Assignee: Ciba-Geigy Corporation
    Inventor: Nalin B. Desai
  • Patent number: 4151291
    Abstract: 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: Grant
    Filed: November 17, 1977
    Date of Patent: April 24, 1979
    Assignee: Unicler
    Inventor: Francois M. J. Vallet
  • Patent number: 4148900
    Abstract: 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: Grant
    Filed: September 16, 1977
    Date of Patent: April 10, 1979
    Assignee: Carlo Erba S.p.A.
    Inventors: Gianfederico Doria, Piernicola Giraldi, Francesco Lauria, Maria L. Corno, Piero Sberze, Marcello Tibolla
  • Patent number: 4144336
    Abstract: 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: Grant
    Filed: July 8, 1976
    Date of Patent: March 13, 1979
    Assignee: Troponwerke Dinklage & Co.
    Inventors: Karl-Heinz Boltze, Peter-Rudolf Seidel, Haireddin Jacobi, Helmut Schwarz
  • Patent number: 4133880
    Abstract: 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: Grant
    Filed: July 28, 1977
    Date of Patent: January 9, 1979
    Assignees: Mitsubishi Chemical Industries Ltd., Shosuke Okamoto
    Inventors: Shosuke Okamoto, Akiko Hijikata, Ryoji Kikumoto, Yoshikuni Tamao, Kazuo Ohkubo, Tohru Tezuka, Shinji Tonomura
  • Patent number: RE30739
    Abstract: 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: Grant
    Filed: May 14, 1979
    Date of Patent: September 8, 1981
    Assignee: Beecham Group Limited
    Inventor: Derek V. Gardner