Chalcogen Or Nitrogen Attached Indirectly To The Hetero Ring By Acyclic Nonionic Bonding Patents (Class 549/407)
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Patent number: 4975454Abstract: Compounds of general formula (I): ##STR1## in which: R.sub.1, R.sub.2, R.sub.3 and R.sub.4, which may be identical or different, denote a hydrogen atom, a halogen atom or a lower alkyl, lower alkenyl, lower alkyloxy or lower alkenyloxy group, optionally substituted with one or more halogen atoms,R.sub.5 denotes a carboxyl, (lower alkyloxy)carbonyl, (lower alkenyloxy)carbonyl or (lower alkynyloxy)-carbonyl,their isomers, stereoisomers and diastereoisomers, and also their addition salts with a pharmaceutically acceptable base.Medicinal products.Type: GrantFiled: April 11, 1989Date of Patent: December 4, 1990Assignee: Adir et CompagnieInventors: Jean-Daniel Brion, Guillaume Le Baut, Patrick Ducrey, Sylvie Piessard-Robert, Claude Cudennec, Genevieve Seurre
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Patent number: 4975451Abstract: Compounds of the formula ##STR1## in which Ar is substituted or unsubstituted phenyl, naphthyl, or thienyl; and Ar.sup.1 is 3-phenoxyphenyl, 4-fluoro-3-phenoxyphenyl, 2-methyl[1-1'-biphenyl]-3-yl, or 6-phenoxy-2-pyridyl, exhibit pyrethroid-like insecticidal and acaricidal activity and are relatively nontoxic to fish.Type: GrantFiled: March 2, 1989Date of Patent: December 4, 1990Assignee: FMC CorporationInventors: Thomas G. Cullen, Scott McN. Sieburth, Gary A. Meier, John F. Engel, Leslie W. Stratton, Alan W. Fritz
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Patent number: 4966983Abstract: 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 16, 1989Date of Patent: October 30, 1990Assignee: BASF AktiengesellschaftInventors: Andreas Guentner, Udo Mayer, Andreas Oberlinner
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Patent number: 4958021Abstract: Benzopyran derivatives of the formula ##STR1## where X is the radical ##STR2## and R.sup.1, R.sup.2, R.sup.3, R.sup.4 and also the ring A have defined meanings are used in pressure- or heat-sensitive layers.Type: GrantFiled: July 19, 1988Date of Patent: September 18, 1990Assignee: BASF AktiengesellschaftInventors: Andreas Guentner, Udo Mayer, Andreas Oberlinner
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Patent number: 4948806Abstract: Certain N-2,6-dialkyl- or N-2,6-dialkoxyphenyl-N'-arylalkylurea compounds are potent inhibitors of the enzyme acyl CoA:cholesterol acyltransferase (ACAT), and are thus useful agents for the treatment of hypercholesterolemia or atherosclerosis.Type: GrantFiled: June 9, 1989Date of Patent: August 14, 1990Assignee: Warner-Lambert CompanyInventor: Bharat K. Trivedi
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Patent number: 4943582Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein: X, Y and R.sub.1 -R.sub.6 are as defined have blood pressure lowering activity and K+ channel activator activity and are useful in the treatment of hypertension.Type: GrantFiled: May 1, 1987Date of Patent: July 24, 1990Assignee: Beecham Group p.l.c.Inventors: John M. Evans, Geoffrey Stemp, Frederick Cassidy
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Patent number: 4942249Abstract: A process for producing alpha-tocopherol and intermediates in this process.Type: GrantFiled: August 17, 1989Date of Patent: July 17, 1990Assignee: Hoffmann-La Roche Inc.Inventor: Noal Cohen
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Patent number: 4931574Abstract: The invention is directed to a process and intermediates for the preparation of benzopyrans such as racemic-6-acetyl-7-[5-(4-acetyl-3-hydroxy-2-propylphenoxy)pentyloxy]-3,4-d ihydro-2H-1-benzopyran-2-carboxylic acid.Type: GrantFiled: August 23, 1988Date of Patent: June 5, 1990Assignee: Hoffmann-La Roche Inc.Inventors: Percy S. Manchand, Robert A. Micheli
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Patent number: 4918092Abstract: Compounds having the formula I: ##STR1## are antagonists of leukotrienes of C.sub.4, D.sub.4 and E.sub.4, the slow reacting substance of anaphylaxis. These compounds are useful as anti-asthmatic, anti-allergic and anti-inflammatory agents.Type: GrantFiled: January 15, 1988Date of Patent: April 17, 1990Assignee: Merck Frosst Canada, Inc.Inventors: Richard Frenette, Robert N. Young, Masatoshi Kakushima
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Patent number: 4897109Abstract: A composition for protecting culture plants from the phytotoxic action of herbicidally active chloracetanilides contains as active ingredient an acylamine derivative of the formula I ##STR1## wherein X is oxygen, sulfur, --SO-- or --SO.sub.2 --,Q is an alkyl, alkenyl, alkinyl group, which may be interupted by oxygen, sulfur, sulfinyl or sulfonyul, or a test 1,3-dioxolan-2-yl-alkyl, 1,3-dioxolan-4-alkyl, 2,2-dialkyl-1,3-dioxolan-4-ylalkyl, 1,3-dioxan-2-ylalkyl, 2-benzopyranylalkyl, alkoxycarbonyl alkenyl-oxycarbonyl or tetrahydrofurylalkyl, or the groupOX represents also a halogenoalkyl radical,n is 1, 2 or 3,Z is hydrogen, halogen, alkyl or dioxymethylene,A is a C.sub.1 -C.sub.8 -hydrocarbon radical which may be staight-chained, branched or cyclic and which is unsubstituted or substituted by alkoxy, alkylthio, cyano or halogen,B is hydrogen, a C.sub.1 -C.sub.Type: GrantFiled: October 5, 1987Date of Patent: January 30, 1990Assignee: Ciba-Geigy CorporationInventor: Henry Martin
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Patent number: 4889871Abstract: This invention encompasses compounds of Formula 1 and the pharmaceutically acceptable salts thereof. ##STR1## wherein R.sup.1 represents alkyl having 2-6 carbon atoms;R.sup.2 represents methyl or ethyl;R.sup.3 represents alkyl having 1 to 5 carbon atoms;W represents (CH.sub.2).sub.x where x is 2 to 7, alkylene having 2 to 7 carbon atoms, alkenylene having 3 to 7 carbon atoms, alkynylene having 3 to 7 carbon atoms, or cyclopentyl;R.sup.4 represents hydrogen, alkyl having 2-5 carbon atoms, alkenyl having 2 to 5 carbon atoms, or alkynyl having 2 to 5 carbon atoms;Q represents oxygen or CH.sub.2 ;B represents CH.sub.2, C.dbd.O or CH--OH;R.sup.5 represents hydrogen, alkyl having 1 to 6 carbon atoms, or R.sup.5 and R.sup.6 together optionally represent a carbon to carbon bond; orR.sup.5 represents alkanoyl having 2 to 4 carbon atoms, carboxy, alkoxycarbonyl, or (CH.sub.2)y--CO.sub.2 R.sup.8 wherein y is 0 to 4 and R.sup.8 is hydrogen or alkyl having 1 to 6 carbon atoms; andA represents --Z--CO.sub.2 R.sup.Type: GrantFiled: May 12, 1988Date of Patent: December 26, 1989Assignee: G. D. Searle & Co.Inventors: Stevan W. Djuric, Robert L. Shone, Stella S. T. Yu
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Patent number: 4885299Abstract: The invention relates to new 2-(2,3-dihydro-2-oxo-3-benzofuranyl)acetic acid compounds of general formula I: ##STR1## in which: R.sub.1 denotes a hydrogen atom, a linear or branched alkyl radical having 1 to 4 carbon atoms or a phenyl radical optionally substituted with a halogen atom or with an alkoxy radical containing 1 to 4 carbon atoms or an alkyl radical having 1 to 4 carbon atoms,R.sub.2 denotes a hydrogen or halogen atom, a hydroxyl radical, an alkyl radical having 1 to 4 carbon atoms or an alkoxy radical containing 1 to 4 carbon atoms,R denotes a hydroxyl radical, a linear or branched alkoxy radical having 1 to 4 carbon atoms, a benzyloxy radical or a radical of general formula A: ##STR2## in which: X and Y, which may be identical or different, each denote a linear or branched alkyl radical containing 1 to 5 carbon atoms, a radical of general formula A.sub.Type: GrantFiled: January 17, 1989Date of Patent: December 5, 1989Assignee: ADIR Et CieInventors: Gilbert Lavielle, Jean Lepagnol
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Patent number: 4882353Abstract: For inhibiting thombocyte aggregation, vasodilating and bronchodilating, the new chroman derivatives of the formula ##STR1## in which R.sup.1 stands for hydrogen, halogen, alkyl, hydroxyl, alkoxy, trifluoromethyl or cyano,R.sup.2 and R.sup.3 are identical or different and stand for hydrogen, alkyl, cycloalkyl or aryl,R.sup.4 stands for hydroxyl, alkoxy, aryloxy, aralkoxy or for a group of the formula --NR.sup.5 R.sup.6, whereR.sup.5 and R.sup.6 are identical or different and in each case denote hydrogen, alkyl, aryl or aralkyl,X denotes a direct bond or an oxygen or sulphur atom, NH or N-alkyl, andn denotes 0 or 1,and their physiologically tolerable salts.Type: GrantFiled: October 26, 1988Date of Patent: November 21, 1989Assignee: Bayer AktiengesellschaftInventors: Ulrich Niewohner, Franz-Peter Hoever, Folker Lieb, Hermann Oediger, Ulrich Rosentreter, Horst Boshagen, Elisabeth Perzborn, Volker-Bernd Fiedler, Friedel Seuter
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Patent number: 4882441Abstract: A process for producing natural vitamin E and intermediates in this process.Type: GrantFiled: September 9, 1988Date of Patent: November 21, 1989Assignee: Hoffmann-La Roche Inc.Inventors: David L. Coffen, Rudolf Schmid, Mark J. Sebastian
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Patent number: 4877890Abstract: A process for producing alpha-tocopherol and intermediates in this process.Type: GrantFiled: October 17, 1988Date of Patent: October 31, 1989Assignee: Hoffmann-La Roche Inc.Inventor: Noal Cohen
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Patent number: 4853472Abstract: A process for producing natural vitamin E and intermediates in this process.Type: GrantFiled: September 9, 1988Date of Patent: August 1, 1989Assignee: Hoffmann-La Roche Inc.Inventors: David L. Coffen, Rudolf Schmid, Mark J. Sebastian
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Patent number: 4841078Abstract: 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: August 9, 1984Date of Patent: June 20, 1989Assignee: Pfizer Inc.Inventors: James F. Eggler, Michael R. Johnson, Lawrence Sherman
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Patent number: 4833259Abstract: The novel sunscreen agents which are esters, namely esters of p-methoxy-cinnamic acid with d,1-.alpha.-tocopherol, pantolactone or panthenol.Type: GrantFiled: August 24, 1987Date of Patent: May 23, 1989Assignee: Hoffmann-La Roche Inc.Inventors: Gustav Erlemann, Christian Fizet, Horst Pauling
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Patent number: 4829080Abstract: An aromatic benzopyranyl or benzothiopyranyl compound of the formula ##STR1## wherein n is 0 or 1,X represents ##STR2## R' represents H, OH, acyloxy or NH.sub.2, R" represents H or alkoxy orR' and R" taken together form an oxo, methano or hydroxyimino radical,R.sub.8 represents H, ##STR3## R.sub.9 represents H, alkyl, mono or polyhydroxyalkyl, aryl, aralkyl, a residue of a sugar or ##STR4## p equals 1, 2 or 3, r' and r" represent H, alkyl, monohydroxyalkyl, polyhydroxyalkyl, aryl, benzyl, the residue of an amino acid or an aminated sugar, or together form a heterocycle,R.sub.1, R.sub.2, R.sub.3 and R.sub.4 represents H or lower alkyl,R.sub.5, R.sub.6 and R.sub.7 represent H or methyl or when n=1, R.sub.5 and R.sub.7 taken together form with the benzene ring a naphthalene ring (R.sub.5 -R.sub.7 .dbd.--CH.dbd.CH--), andthe salts of said compounds as well as their geometric and optical isomers.These compounds are useful in pharmaceutical and cosmetic compositions.Type: GrantFiled: March 12, 1987Date of Patent: May 9, 1989Assignee: L'OrealInventors: Jean Maignan, Gerard Lang, Gerard Malle, Serge Restle, Braham Shroot
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Patent number: 4826984Abstract: Novel heteroarotinoid compositions characterized by the formulae: ##STR1## where R is H, CH.sub.3 or C.sub.2 H.sub.5 and X is S, S O, O, NCH.sub.3, Si(CH.sub.3).sub.2, N.sup.+ (H)CH.sub.3 [Cl.sup.- ], N.sup.+ (H)CH.sub.3 [Br.sup.- ] or N.sup.+ (alkyl) CH.sub.3 [Cl.sup.- or Br.sup.-) where alkyl is CH.sub.3, C.sub.2 H.sub.5, CH.sub.2 .dbd.CHCH.sub.2 or C.sub.6 H.sub.5 CH.sub.2. Such compositions exhibit activity as anticancer agents.Type: GrantFiled: January 27, 1987Date of Patent: May 2, 1989Assignee: The Board of Regents for the Oklahoma Agricultural and Mechanical College acting for and on behalf of Oklahoma State UniversityInventors: Kenneth D. Berlin, Elizabeth M. Holt, Warren T. Ford, Mark D. Thompson
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Patent number: 4810804Abstract: Retinoid-like activity is exhibited by compounds of the formula ##STR1## where X is S, O or NR.sub.1 where R.sub.1 is hydrogen or lower alkyl; n is 0-5; R is H or lower alkyl and A is H, --COOH or a pharmaceutically acceptable salt, ester or amide thereof, --CH.sub.2 OH or an ether or ester derivative thereof, or --CHO or an acetal derivative thereof, or --COR.sub.2 or a ketal derivative thereof where R.sub.2 is --(CH.sub.2).sub.m CH.sub.3 where m is 0-4; or a pharmaceutically acceptable salt.Type: GrantFiled: March 26, 1987Date of Patent: March 7, 1989Assignee: Allergan, Inc.Inventor: Roshantha A. S. Chandraratna
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Patent number: 4806661Abstract: Novel 2-halochromans and their coupling to various nucleophiles to produce Vitamin E and as well as novel intermediates for Vitamin E.Type: GrantFiled: January 21, 1988Date of Patent: February 21, 1989Assignee: Hoffmann-La Roche Inc.Inventor: Noal Cohen
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Patent number: 4804684Abstract: Drugs with high anticonvulsant and analgesic activities constituted by symmetrical .beta.-dialkoxyiminocycloalklene derivatives in which the imine double bonds are conjugated with the cyclic double bond or bonds belonging to one or more fused benzene rings.Type: GrantFiled: January 20, 1987Date of Patent: February 14, 1989Assignee: Panmedica S.A.Inventors: Claude Laruelle, Marcel Lepant, Bernard Raynier
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Patent number: 4801724Abstract: A process for producing alpha-tocopherol and intermediates in this process.Type: GrantFiled: June 5, 1987Date of Patent: January 31, 1989Assignee: Hoffmann-La Roche Inc.Inventor: Noal Cohen
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Patent number: 4789750Abstract: 6-Etherified hydroxy -2-(4',8',12'-trimethyl-5'-tridecenyl)-2,5,7,8-tetramethylchromans with an oxo or hydroxy substituent at the 2' position which may be substituted with an arylsulfonyl or a carboxyalkyl at the 3' position and containing a single or double bond at the 11 position, said chromans being intermediates for producing natural vitamin E.Type: GrantFiled: March 27, 1987Date of Patent: December 6, 1988Assignee: Hoffman-La Roche Inc.Inventors: David L. Coffen, Rudolf Schmid, Mark J. Sebastian
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Patent number: 4785017Abstract: The invention relates to compounds of the formula ##STR1## wherein R.sup.1 is hydrogen or lower alkyl; R.sup.2 is hydrogen or halogen; R.sup.3, R.sup.4 and R.sup.5 are hydrogen, acyl or lower alkyl; R.sup.6 and R.sup.7, independently, are hydrogen or lower alkyl; X is alkylene.sub.3-7 ; and n is an integer of zero to four; provided that only one of R.sup.3, R.sup.4 or R.sup.5 can be acyl;enantiomers thereof, and, when R.sup.7 is hydrogen, salts thereof with pharmaceutically acceptable bases.The compounds of formulas I and II are useful as agents for the treatment of allergic conditions.Type: GrantFiled: May 29, 1984Date of Patent: November 15, 1988Assignee: Hoffmann-La Roche Inc.Inventors: Noal Cohen, Giuseppe F. Weber
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Patent number: 4778903Abstract: The invention relates to compounds of the formula: ##STR1## which are useful as leukotriene D.sub.4 (LTD.sub.4) inhibitors and therefore useful in the treatment of allergies and inflammatory conditions.Type: GrantFiled: December 12, 1984Date of Patent: October 18, 1988Assignee: G. D. Searle & Co.Inventors: Masateru Miyano, Robert L. Shone, Daniel D. Sohn
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Patent number: 4742077Abstract: Compounds of formula I ##STR1## wherein R.sub.1 represents a group of formula ##STR2## whereby R.sub.4 and R.sub.5 are the same or different and represent hydrogen, halogen, lower alkyl, lower alkoxy or trifluoromethyl and X represents oxygen, sulfur, imino, lower alkylimino, --(CH.sub.2)--, --(S.CH.sub.2)-- or --(O.CH.sub.2)--,R.sub.2 represents hydrogen or lower alkyl,R.sub.3 represents a group of formula ##STR3## whereby R.sub.6, R.sub.7 and R.sub.8 are the same or different and represent hydrogen or alkyl or R.sub.6 together with R.sub.7 or R.sub.7 together with R.sub.8 represent --(CH.sub.2).sub.m -- wherein m is 3 to 6,R.sub.9 represents alkyl, alkenyl, trialkylsilyl or alkyl substituted by hydroxy, lower alkoxy, lower halogenalkyl or aryl andn stands for 1, 2 or 3,which possess pharmaceutical in particular antimycotic activity as well as activity against phytopathogenic fungi.Type: GrantFiled: September 8, 1986Date of Patent: May 3, 1988Assignee: Sandoz Ltd.Inventor: Anton Stutz
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Patent number: 4728650Abstract: There are provided novel 3,4-dihydrobenzopyran derivatives having anti-peptic ulcer, antitussive and/or expectorant activity. Also provided are medicinal uses of said 3,4-dihydrobenzopyran derivatives.Type: GrantFiled: May 13, 1986Date of Patent: March 1, 1988Assignee: Kuraray Co., Ltd.Inventors: Katsushi Eziri, Koichi Kanehira, Manzo Shiono, Yoshiji Fujita, Johji Yamahara
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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: 4694090Abstract: Novel chroman compounds which have excellent antioxidant activity and/or analgesic activity or serve as precursors for such active compounds are provided. There are also provided uses of these active compounds as an antioxidant and/or analgesic.Type: GrantFiled: December 7, 1984Date of Patent: September 15, 1987Assignee: Kuraray Co., Ltd.Inventors: Manzo Shiono, Yoshiji Fujita, Takashi Nishida
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Patent number: 4684661Abstract: The invention relates to novel homopropargylamines of formula I ##STR1## wherein n is 2 or 3,R.sub.1 is a group of formula IIa, IIb or IIc ##STR2## in which R.sub.6 and R.sub.7 independently are H, halogen, CF.sub.3, lower alkyl or lower alkoxy,s is a number of 3 to 5,X is O, S, OCH.sub.2, SCH.sub.2, CH.sub.2 or NR.sub.8, andR.sub.8 is H or lower alkyl,R.sub.2 is H or lower alkyl, eitherR.sub.3 and R.sub.4, independently, are H or lower alkyl, orR.sub.3 and R.sub.4 together are (CH.sub.2).sub.u, in which u is a number of 3 to 5, andR.sub.5 is H, alkenyl or is a group selected from alkyl, trialkylsilyl, dialkylphenylsilyl, phenyl, phenylalkyl and cycloalkyl, in which alkyl, phenyl and cycloalkyl groups or moieties are unsubstituted or substituted by OH, lower alkyl, lower alkoxy, phenyl or halogen,in free base form or acid addition salt form thereof, their preparation, their chemotherapeutical and agricultural use and to compositions comprising such novel compounds and suitable for such use.Type: GrantFiled: November 20, 1985Date of Patent: August 4, 1987Assignee: Sandoz Ltd.Inventor: Anton Stuetz
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Patent number: 4677211Abstract: 7-Substituted lower alkyl hept-6-enoates and 4-hydroxytetrahydropyran-2-ones bearing 6-olefinic substituents (e.g.,) ethyl erythro-3,5-dihydroxy-7-phenyl-hept-6-enoates are prepared by a multi-step process. The process involves 3-protected-lower alkyl 3,5-dihydroxy-hept-6-enoates, which are obtained by cleaving corresponding 6.alpha.-vinyl-4.beta.-protected hydroxy-tetrahydro 2H-pyran-2-ones. The final products are useful as anti hypercholesteremic agents.Type: GrantFiled: July 26, 1985Date of Patent: June 30, 1987Assignee: Sandoz Pharmaceuticals Corp.Inventors: Charles F. Jewell, Jr., James R. Wareing
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Patent number: 4659737Abstract: Substituted benzopyrans of the formula ##STR1## in which --A-- is a single or double bond,X is a direct bond, optionally substituted methylene, oxygen or optionally substituted --NH--, and the various other radicals can have various meanings,or pharmaceutically acceptable addition salts thereof, which possess anti-hypertensive activity.Type: GrantFiled: March 25, 1985Date of Patent: April 21, 1987Assignee: Bayer AktiengesellschaftInventors: Hans-Joachim Kabbe, Ulrich Niewohner, Arno Widdig, Andreas Knorr, Bernward Garthoff, Stanislav Kazda
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Patent number: 4654362Abstract: Derivatives of 2,2'-iminobisethanol having useful properties in the treatment and/or the prevention of disorders of the coronary-vascular system.Type: GrantFiled: October 12, 1984Date of Patent: March 31, 1987Assignee: Janssen Pharmaceutica, N.V.Inventors: Guy R. E. Van Lommen, Marcel F. L. De Bruyn, Marc F. J. Schroven
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Patent number: 4645845Abstract: Novel optically active chroman derivatives of the general formulae Ia and Ib ##STR1## where R.sup.1, R.sup.2, R.sup.3 and R.sup.Type: GrantFiled: March 12, 1984Date of Patent: February 24, 1987Assignee: BASF AktiengesellschaftInventors: Henning-Peter Gehrken, Hansgeorg Ernst, Joachim Paust
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Patent number: 4617407Abstract: Compounds having the formula: ##STR1## are antagonists of leukotrienes of C.sub.4, D.sub.4 and E.sub.4, the slow reacting substance of anaphylaxis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.Type: GrantFiled: August 30, 1984Date of Patent: October 14, 1986Assignee: Merck Frosst Canada, Inc.Inventors: Robert N. Young, Joshua Rokach
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Patent number: 4610983Abstract: This invention relates to a novel N-acyl acidic amino acid diamide derivative represented by the general formula or a salt thereof: ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4, which may be the same or different, represents a hydrogen atom or a substituted or unsubstituted alkyl, cycloalkyl, alkenyl or aralkyl group, or R.sup.1 and R.sup.2 and/or R.sup.3 and R.sup.4, when taken together with the respective adjacent nitrogen atoms, form a substituted or unsubstituted heterocyclic group; R.sup.5 represents a substituted or unsubstituted cycloalkyl, acyl or heterocyclic group; A represents a bond or a substituted or unsubstituted alkylene, alkenylene or alkadienylene group; and n is 1, 2 or 3. Said compound has an anti-ulcer activity which is effective to human beings and animals. This disclosure relates to such a compound, to a process for the production thereof and to an anti-ulcer agent containing the same.Type: GrantFiled: December 3, 1984Date of Patent: September 9, 1986Assignee: Toyama Chemical Co., Ltd.Inventors: Noboru Takagawa, Shiro Hirai, Takuya Kodama, Hiroshi Hirano, Yasuo Kiba, Mikio Kawabata, Tatsuya Miyaura, Yasuyuki Suzuki
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2,4-diamino-(substituted-benzopyran(quinolyl,isoquinoly)methyl)pyrimidine s useful as antibacterials
Patent number: 4587342Abstract: Novel 2,4-diaminopyrimidines having substituted heterobicyclomethyl moieties in the 5-position have superior antibacterial properties.Type: GrantFiled: October 31, 1983Date of Patent: May 6, 1986Inventors: Susan M. Daluge, Paul M. Skonezny -
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: 4563458Abstract: The invention relates to substituted 4-aminomethylene-chromans and chromens of Formula (I) infra, as well as methods for making of said chromans and chromens, compositions containing said chromans and chromens and methods for the use of said chromans, chromens and compositions containing said chromans and chromens. The compounds and compositions of the invention are useful for their circulation influencing activity.Type: GrantFiled: December 13, 1983Date of Patent: January 7, 1986Assignee: Bayer AktiengesellschaftInventors: Arno Widdig, Hans-Joachim Kabbe, Andreas Knorr, Ulrich Benz
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Patent number: 4547579Abstract: There are described novel dyes of the formulae ##STR1## in which R.sub.1 and R.sub.2 independently of one another are each hydrogen, unsubstituted or substituted alkyl, cycloalkyl, aralkyl or aryl, and R.sub.1 and R.sub.2 together with the nitrogen atom, and optionally with the inclusion of further hetero atoms, can also form a 5- to 7-membered heterocycle, or one of the radicals R.sub.1 or R.sub.2 can be linked with the carbon atoms, in the o-position with respect to the amino group, of the ring A to form a fused-on, saturated, unsubstituted or substituted 5- or 6- membered ring,X is .dbd.NR.sub.3, .dbd.NCOR.sub.4, ##STR2## .dbd.NH or .dbd.O, wherein R.sub.3 is alkyl or unsubstituted or substituted phenyl,R.sub.4 is unsubstituted or substituted alkyl, aralkyl, aryl, vinyl, alkoxy, phenoxy or amino, andR.sub.5 is cyano, carbalkoxy, or unsubstituted or substituted carbonamide, andR.sub.Type: GrantFiled: September 30, 1982Date of Patent: October 15, 1985Assignee: Ciba-Geigy CorporationInventor: Peter Mockli
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Patent number: 4544758Abstract: The invention relates to intermediate compounds having the general formula I ##STR1## in which R.sup.1 is H, an alkyl, arylalkyl or an aliphatic acyl radical, preferably a benzyl or acetyl group and wherein X and Y together span an additional bond between the X and Y carrying C atoms (Ia) or in which Y is OH and X is H (Ib) and in which the dotted line can represent an additional bond particularly [2R,1'Z,3'E,7'E]-6-benzyloxy-2,5,7,8-tetramethyl-2-(4',8',12'-trimethyl-tr ideca-1',3',7'-trien-1'-yl)chroman and 6-benzyloxy-2,5,7,8-tetramethyl-2-(1'-hydroxy-4',8',12'-trimethyl-trideca- 3',7'-diene-1'-yl)chroman, as well as compounds and methods of preparing compounds having the general formula II ##STR2## in which Z is one of the groups ##STR3## wherein R.sup.2 is an alkyl group with 1 to 4 carbon atoms preferably CH.sub.3 or C.sub.2 H.sub.Type: GrantFiled: June 28, 1983Date of Patent: October 1, 1985Assignee: Basf AktiengesellschaftInventors: Friedrich Vogel, Joachim Paust, Axel Nuerrenbach
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Patent number: 4523024Abstract: There is provided a class of novel 3,4-dihydro-2H-benzopyran derivatives which either have excellent inhibitory activity against unfavorable effects of heat, light and oxidative factors or are of use as precursors of compounds having such activity, and methods for producing these derivatives. Also provided are methods of using such 3,4-dihydro-2H-benzopyran derivatives as stabilizers for organic materials sensitive to heat, light or/and oxidative factors, and organic compositions containing such stabilizers.Type: GrantFiled: November 15, 1983Date of Patent: June 11, 1985Assignee: Kuraray Co., Ltd.Inventors: Manzo Shiono, Yoshiji Fujita, Takashi Nishida
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Patent number: 4515975Abstract: Chroman derivatives of the general formula I ##STR1## where A--B is --CH.sub.2 --CH.sub.2 --(Ia), --CH.dbd.CH--(Ib), --CHOH--CH.sub.2 --(Ic) or --CO--CH.sub.2 --(Id), R.sup.1 is --CH.sub.2 --O--R' or ##STR2## where R' is C.sub.1 -C.sub.4 -alkyl or arylmethyl and R" and R'" are each C.sub.1 -C.sub.4 -alkyl, which can also be bonded to form a five-membered or six-membered cyclic acetal, R.sup.2 is C.sub.1 -C.sub.4 -alkyl and R.sup.3 is H or a protective group.Type: GrantFiled: November 4, 1982Date of Patent: May 7, 1985Assignee: BASF AktiengesellschaftInventors: Friedrich Vogel, Joachim Paust
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Patent number: 4511685Abstract: Chroman derivatives of the general formula I ##STR1## where R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are each H or C.sub.1 -C.sub.4 -alkyl, R.sup.5 is C.sub.10 -C.sub.30 -alkyl or C.sub.10 -C.sub.30 -alkenyl, X and Y are each O, NH or S, m is 0, 1, 2 or 3 and n and r are each 0 or 1, the preparation of compounds I by various methods known per se, and the use of the compounds as stabilizers for organic materials.Type: GrantFiled: February 26, 1981Date of Patent: April 16, 1985Assignee: BASF AktiengesellschaftInventors: Axel Nissen, Michael Horner, Dieter Horn, Erik Lueddecke, Gernot Teege
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Patent number: 4506079Abstract: Convenient intermediates for preparing 3-substituted-2-hydroxypropyl aryl ether .beta.-blockers, a reaction to the intermediates of the following formula and a conversion to obtain the said .beta.-blockers are disclosed. ##STR1## (wherein X is hydrogen or halogen;Y is halogen, hydroxy, lower acyloxy, amino, lower alkylamino, lower aralkylamino, lower acylamino, di-lower alkylamino, lower alkyleneamino, N-lower alkyl-N-lower aralkylamino, di-lower acylamino, N-lower alkyl-N-lower acylamino or N-tri-lower alkylsilylamino;one of P and R combined together with Q represents lower alkylene or alkenylene optionally interrupted by O, N or S and optionally substituted by lower alkyl, lower aralkyl, lower carboxylic acyl, carboxy, protected carboxy; hydroxy, lower alkoxy, lower acyloxy, oxo; amino, lower alkylamino, lower acylamino, nitro, nitroso, lower alkylthio, lower sulfonic acyl or halogen;and the remaining R or P is hydrogen or halogen;and dotted line represents the presence of one or two double bonds).Type: GrantFiled: March 5, 1980Date of Patent: March 19, 1985Assignee: Shionogi & Co., Ltd.Inventor: Makiko Sakai
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Patent number: 4503066Abstract: The invention provides various medical compositions for use in treating or preventing certain of the side effects of diabetes or galactosemia. The active ingredients are selected from a series of novel aldose reductase inhibitory spiro-linked pyrrolidine-2,5-diones of the general formula: ##STR1## or a pharmaceutically acceptable salt, or a non-toxic, biodegradable precursor thereof. Processes for the production of these compounds are also provided. A particular compound suitable for use as an active ingredient is spiro[pyrrolidine-3,9'-xanthene]-2,5-dione.Type: GrantFiled: May 11, 1982Date of Patent: March 5, 1985Assignee: Imperial Chemical Industries PLCInventors: David R. Brittain, Robin Wood
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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.