Acyclic Chalcogen Bonded Directly To Ring Carbon Of The Bicyclo Ring System Patents (Class 546/116)
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Patent number: 5077407Abstract: The present invention provides novel substituted 2-[monoannelated(3,4- 4,5-, and 5,6-)pyridylalkylenesulfinyl]-benzimidazoles with gastric acid inhibiting effects.Type: GrantFiled: October 31, 1988Date of Patent: December 31, 1991Assignee: The Upjohn CompanyInventor: John C. Sih
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Patent number: 5071871Abstract: New benz[b]pyranes and pyranopyridines of formula I, ##STR1## wherein the significances of substituents V, T, W, R.sub.3 to R.sub.5, R.sub.9, R.sub.10, m, X, Y and Z are given in claim 1 and their N-oxides and their salts and their use in the treatment of raised blood pressure in the treatment of vascular disorders and other disorders in which a reduction in tension of the smooth muscles is therapeutically useful, as well as in the treatment of hair loss and baldness. Further the compounds are useful in the treatment of asthma and obstructive disorders of the respiratory system as well as in the prophylactic treatment of obstructive or inflammatory airways disease, for example asthma, as well as novel pharmaceutical compositions comprising said K.sup.+ channel activators suitable for such use.Type: GrantFiled: July 10, 1990Date of Patent: December 10, 1991Assignee: Sandoz Ltd.Inventors: Stefan Blarer, John Morley, Ian D. Chapman
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Patent number: 5071986Abstract: Chromogenic phthalides and azaphthalides of the formula ##STR1## in which V.sub.1 and V.sub.2 are each, independently of the other, hydrogen, halogen, lower alkyl, lower alkoxy, (lower)alkoxycarbonyl or --NR.sub.1 R.sub.2, at least one of the radicals V.sub.1 and V.sub.2 being lower alkoxy or --NR.sub.1 R.sub.2, A is an unsubstituted or halogen-, cyano-, nitro-, (lower alkyl)-, (lower alkoxy)-, (lower alkyl)thio-, (lower alkyl)amino- or di(lower) alkyl)amino-substituted benzene, naphthalene, pyridine, quinoline, pyrazine or quinozaline ring, B is a substituted phenyl radical of the formula ##STR2## or a 3-indolyl of the formula ##STR3## Q is ##STR4## --S-- or --O--, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are each, independently of the others, hydrogen, unsubstituted or halogen-, hydroxy-, cyano- or (lower alkoxy)-substituted alkyl, cycloalkyl or unsubstituted or ringsubstituted phenalkyl or phenyl, or the substituent pairs (R.sub.1 and R.sub.2) and (R.sub.3 and R.sub.Type: GrantFiled: November 30, 1990Date of Patent: December 10, 1991Assignee: Ciba-Geigy CorporationInventors: Rox Phaff, Davor Bedekovic
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Patent number: 5071868Abstract: A process for the preparation of S- or R-carbazole derivatives of the general formula: ##STR1## in which R is an unsubstituted or substituted amino radical and pharmacologically acceptable salts, by either reacting R-(-)-epichlorohydrin (for the S-carbozole derivative); or reacting an S-epoxide derivative of the general formula: ##STR2## in which R.sub.1 is the residue of a substituted sulphonic acid derivative (for the R-carbazole derivative); with 4-hydroxycarbazole and then with ammonia or a substituted amine of the general formula RH, and recovering the compound or converting it to a pharmacologically acceptable salt.The new R-(+)- and S(-)-carbazole derivatives provided by the inventive process have unexpected beta blocking and vasodilatory properties and are useful in pharmaceutical compositions. R-(+)-carbazole derivatives are also useful for the treatment of glaucoma.Type: GrantFiled: January 28, 1991Date of Patent: December 10, 1991Assignee: Boehringer Mannheim GmbHInventor: Herbert Leinert
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Patent number: 5068333Abstract: The present invention relates to processes and intermediates for the preparation of spiro-heteroazolones. The latter compounds are useful as aldose reductase inhibitors.Type: GrantFiled: March 7, 1990Date of Patent: November 26, 1991Assignee: Pfizer Inc.Inventors: Charles W. Murtiashaw, George J. Quallich
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Patent number: 5062881Abstract: 2-(1-Substituted-2-imidazolin-2-yl)benzoic and nicotinic acids, and derivatives thereof, which are effective in the control of undesirable plant species are described. Also described are a method for the herbicidal use of the compounds and a method for their preparation.Type: GrantFiled: December 20, 1989Date of Patent: November 5, 1991Assignee: American Cyanamid CompanyInventor: Michael A. Guaciaro
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Patent number: 5061713Abstract: Compound of general formula (I): ##STR1## in which: X, Y, Z and T each represent, independently of one another, a nitrogen atom, a --CH.dbd. group or a group CW, in which W represents a halogen atom or a lower alkyl or alkoxy group optionally substituted with one or more halogen atoms, such as a trifluoromethyl group, on condition that only one of them represents a nitrogen atom,Ra, Rb, Rc, Rd and Re represent, independently of one another, a hydrogen atom, a halogen atom or a lower alkyl or alkoxy group optionally substituted with one or more halogen atoms, such as a trifluoromethyl group,B represents a hydrogen atom and D a hydroxyl group, or B and D simultaneously represent an oxygen atom,n represents 1 or 2, andR.sub.Type: GrantFiled: August 7, 1990Date of Patent: October 29, 1991Assignee: Science et OrganizationInventors: Gerald Guillaumet, Christine Flouzat, Jacqueline Bonnet
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Patent number: 5047537Abstract: This invention relates to a method for the separation of stereoisomers of 7-hydroxy-furo[3,4-c]pyridine derivatives of the formula ##STR1## wherein R.sub.3, R.sub.4 and R.sub.6 represent various substitutents, which comprises reacting a fully O-acetylated monosaccharide halogenide with a racemate of the selected 7-hydroxy-furo[3,4-c]pyridine derivative, to form the (+) and (-) (O-acetylated monosaccharide) (furo[3,4-c] pyridine 7-yl derivative) ethers, then separating the (+) and the (-) ethers by selective crystallization, in an hydroalcoholic medium, either of the acetylated forms or of the corresponding desacetylated forms and, finally, working up each of the separated derivatives by the usual routes. The compounds are known pharmaceuticals.Type: GrantFiled: October 18, 1990Date of Patent: September 10, 1991Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)Inventors: Andre Esanu, Charles Eck
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Patent number: 5043448Abstract: The invention relates to a method for the preparation of a non-racemic furo [3,4-c] pyridine derivatives of the formula I ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 stand for various substitutents, comprising adding a concentrated strong acid to a solution of a non-racemic compound of the formula II ##STR2## in an amount sufficient to catalyze a deprotection/cyclodehydration. These compounds are known antihypertensives.Type: GrantFiled: July 26, 1990Date of Patent: August 27, 1991Assignee: Societe de Conseils de Recherches et d'Applications ScientifiquesInventor: Charles Eck
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Patent number: 5034531Abstract: Novel polycyclic pyranyl compounds, pharmaceutical compositions, and their use as anti-viral agents are disclosed.Type: GrantFiled: December 23, 1988Date of Patent: July 23, 1991Assignee: Schering CorporationInventors: Richard J. Friary, John H. Schwerdt, Ashit K. Ganguly
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Patent number: 5026713Abstract: Novel compounds represented by the formula: ##STR1## wherein R represents hydrogen, optionally substituted alkyl radicals having from 1 to about 10 carbon atoms, optionally substituted alkenyl radicals having from 1 to about 10 carbon atoms, optionally substituted aryl, alkaryl and aralkyl radicals having from about 6 to about 16 carbon atoms and optionally substituted acyl and acyloxy radicals having from about 1 to about 10 carbon atoms, manifest glycosidase inhibition activity.Type: GrantFiled: August 29, 1989Date of Patent: June 25, 1991Assignee: Monsanto CompanyInventors: Daniel P. Getman, Gary A. DeCrescenzo
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Patent number: 5026714Abstract: Novel blood sugar-lowering dihydropyridinelactones of the formula ##STR1## in which R represents halogen, C.sub.1 -C.sub.10 -alkyl, C.sub.1 -C.sub.10 -alkoxy, C.sub.1 -C.sub.10 -alkylthio, C.sub.1 -C.sub.10 -alkylsulphinyl, C.sub.1 -C.sub.10 -alkylsulphonyl, cyano, C.sub.1 -C.sub.6 - mono- or polyfluoroalkyl, C.sub.1 -C.sub.6 -mono- or polyfluoroalkoxy or nitro,R.sup.1 represents hydrogen, halogen or C.sub.1 -C.sub.10 -alkyl or C.sub.1 -C.sub.10 -alkoxy,R.sup.2 represents a C.sub.1 -C.sub.20 hydrocarbon radical which can optionally be interrupted or substituted,R.sup.3 represents hydrogen NH.sub.2, CHO, CN or a C.sub.1 -C.sub.6 hydrocarbon radical which can be interrupted in the chain, andR.sup.4 represents a C.sub.1 -C.sub.10 -alkyl or C.sub.2 -C.sub.10 -alkenyl radical which can optionally be interrupted or substituted with the proviso that R is not CF.sub.3 if R.sup.2 represents C.sub.2 H.sub.5.Type: GrantFiled: November 13, 1989Date of Patent: June 25, 1991Assignee: Bayer AktiengesellschaftInventors: Siegfried Goldmann, Friedrich Bossert, Hilmar Bischoff, Dieter Petzinna, Walter Puls, Klaus Schlossmann
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Patent number: 5026855Abstract: The present invention relates to stereospecific processes for the preparation of enantiomers of 3-substituted-furo[3,4-c]pyridine of formula I, wherein R.sub.3, R.sub.4 and R.sub.6 stand for various substituents, comprising the steps of: oxidation of a racemic pyridine derivative of formula II, reduction of the resulting ketone with a reducing agent, sterospecific locking or blocking of the OH group of the enantiomer alcohol, opening of the acetonide ring and cyclization of the resulting compound. ##STR1##The present invention also relates to compounds thus obtained and therapeutical compositions thereof.Type: GrantFiled: November 28, 1989Date of Patent: June 25, 1991Assignee: Societe de Consels de Recherches et d'Applications ScientifiquesInventors: Marc Bonato, Charles Eck
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Patent number: 5025021Abstract: Novel compounds represented by the formula: ##STR1## wherein R represents hydrogen, optionally substituted alkyl radicals having from 1 to about 10 carbon atoms, optionally substituted alkenyl radicals having from 1 to about 10 carbon atoms, optionally substituted aryl, alkaryl and aralkyl radicals having from about 6 to about 16 carbon atoms and optionally substituted acyl and acyloxy radicals having from about 1 to about 10 carbon atoms, manifest glycosidase inhibition activity.Type: GrantFiled: July 27, 1989Date of Patent: June 18, 1991Assignee: Monsanto CompanyInventors: Daniel P. Getman, Gary A. DeCrescenzo
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Patent number: 5004813Abstract: Chromogenic phthalides and azaphthalides of the formula ##STR1## in which V.sub.1 and V.sub.2 are each, independently of the other, hydrogen, halogen, lower alkyl, lower alkoxy, (lower alkoxy)carbonyl or --NR.sub.1 R.sub.2, at least one of the radicals V.sub.1 and V.sub.2 being lower alkoxy or --NR.sub.1 R.sub.2, A is an unsubstituted or halogen-, cyano-, nitro-, (lower alkyl)-, (lower alkoxy)-, (lower alkyl)thio-, (lower alkyl)amino- or di(lower alkyl)amino-substituted benzene, naphthalene, pyridine, quinoline, pyrazine or quinoxaline ring, B is a substituted phenyl radical of the formula ##STR2## or a 3-indolyl of the formula ##STR3## Q is ##STR4## --S-- or --O--, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are each, independently of the others, hydrogen, unsubstituted or halogen-, hydroxy-, cyano- or (lower alkoxy)-substituted alkyl, cycloalkyl or unsubstituted or ringsubstituted phenalkyl or phenyl, or the substituent pairs (R.sub.1 and R.sub.2) and (R.sub.3 and R.sub.Type: GrantFiled: August 24, 1989Date of Patent: April 2, 1991Assignee: Ciba-Geigy CorporationInventors: Rox Phaff, Davor Bedekovic
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Patent number: 5003072Abstract: O-acylated derivatives of 1,5-dideoxy-1,5-imino-D-glucitol and their N-alkyl, N-acyl and N-aryl derivatives in which from one to four of the free hydroxyl groups are acylated with acyl groups having from one to eight carbon atoms and in which the N-alkyl and N-acyl substituents contain from four to fourteen carbon atoms and the N-aryl substituents contain from seven to fourteen carbon atoms are disclosed, provided that when N-aryl is benzyloxycarbonyl, the O-acyl groups contain four to eight carbon atoms.Type: GrantFiled: October 12, 1989Date of Patent: March 26, 1991Assignee: G. D. Searle & Co.Inventors: Richard A. Partis, Francis J. Koszyk, Richard A. Mueller
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Patent number: 5002957Abstract: Azaneophyl and silazaneophyl sulfides, processes for their preparation, agents containing them, and their use as pesticides.Compounds of the formula I, their optical isomers and mixtures thereof ##STR1## where M denotes C or Si,R.sup.1 denotes unsubstituted or substituted pyridyl, unsubstituted or substituted pyrimidyl, andwhen M=C- denotes unsubstituted or substituted pyridazinyl, unsubstituted or substituted pyrazinyl, unsubstituted or substituted 1,2,4-triazinyl, unsubstituted or substituted 1,2,4,5-tetrazinyl,R.sup.2, R.sup.3 independently or one another denote alkyl, alkenyl, haloalkyl, phenyl, or R.sup.2 and R.sup.3 denote an alkylene chain which - together with the quaternary central atom (M) - form an unsubstituted or fluorine-substituted ring having four to six ring members (when M=Si) or having three to six ring members (when M=C),R.sup.4 denotes H, F, --CN, --CCl.sub.3, --C.dbd.CH, (C.sub.1 -C.sub.4)alkyl, ##STR2## R.sup.Type: GrantFiled: March 23, 1989Date of Patent: March 26, 1991Assignee: Hoechst AktiengesellschaftInventors: Hans H. Schubert, Gerhard Salbeck, Hans-Peter Krause, Werner Knauf, Anna Waltersdorfer, Manfred Kern
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Patent number: 5001130Abstract: A series of psychotropic heterobicycloalkylpiperazine derivatives having the structure ##STR1## wherein V is a 3- or 4-membered unsaturated chain, containing all carbon atoms when 4-membered, or when a 3-membered chain, V contains an oxygen or sulfur atom as one of the members; R is H or C.sub.1-4 alkyl; W is CH, N, CH.sub.2, or a chemical bond; X is CH, N, SO.sub.2, or CO, with the proviso that both W and X cannot simultaneously be N; and Z is a heteroaromatic ring system. These compounds are useful antipsychotic and/or anxiolytic agents.Type: GrantFiled: February 18, 1988Date of Patent: March 19, 1991Assignee: Bristol-Myers CompanyInventors: James S. New, William L. Christopher
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Patent number: 4996204Abstract: A series of novel 6-substituted-5-oxo-6H-pyrido[2,3-d]pyridazine-8-ylacetic acid and 7-substituted-8-oxo-7H-pyrido[2,3-d]pyridazine-5-ylacetic acid compounds have been prepared, including their C.sub.1 -C.sub.6 alkyl ester derivatives, as well as the base salts of said acids with pharmacologically acceptable cations. Typical member compounds include those acids wherein the ring substitutent is always attached to the available ring-nitrogen atom and is either a lower aralkyl group or a lower heteroaralkyl group. These compounds are useful in therapy as aldose reductase inhibitors for the control of certain chronic diabetic complications. Methods for preparing these compounds from known starting materials are provided.Type: GrantFiled: May 11, 1989Date of Patent: February 26, 1991Assignee: Pfizer Inc.Inventors: Banavara L. Mylari, William J. Zembrowski
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Patent number: 4996320Abstract: A pyridine-compound is reacted with fluorine together with a Bronsted acid-compound or Lewis acid to form a N-fluoropyridinium salt which is very active to other compounds but is very selective for the preparation of a desired product and this product is very useful for a fluorine-introducing agent which makes it useful for the preparation of fluoro-compounds such as thyroid inhibitor.Type: GrantFiled: January 9, 1989Date of Patent: February 26, 1991Assignee: Sagami Chemical Research CenterInventors: Teruo Umemoto, Kyoichi Tomita, Kosuke Kawada, Ginjiro Tomizawa
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Patent number: 4985454Abstract: A process for the preparation of S- or R-carbazole derivatives of the general formula: ##STR1## in which R is an unsubstituted or substituted amino radical and pharmacologically acceptable salts, by either reacting R-(-)-epichlorohydrin (for the S-carbazole derivative); or reacting an S-epoxide derivative of the general formula: ##STR2## in which R.sub.1 is the residue of a substituted sulphonic acid derivative (for the R-carbazole derivative); with 4-hydroxycarbazole and then with ammonia or a substituted amine of the general formula RH, and recovering the compound or converting it to a pharmacologically acceptable salt.The new R-(+)- and S(-)-carbazole derivatives provided by the inventive process have unexpected beta blocking and vasodilatory properties and are useful in pharmaceutical compositions. R-(+)-carbazole derivatives are also useful for the treatment of glaucoma.Type: GrantFiled: January 19, 1989Date of Patent: January 15, 1991Assignee: Boehringer Mannheim GmbHInventor: Herbert Leinert
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Patent number: 4980345Abstract: There are disclosed a pyrazole compound represented by the formula, ##STR1## wherein the substituents of R.sub.1 to R.sub.7 and the sumbol Z have the specified meanings as described in the text, an insecticidal, acaricidal and fungicidal composition containing the same, use of said composition for control of insects, acarids and fungi and a method of preparing said compound, and its intermediate.Type: GrantFiled: September 21, 1989Date of Patent: December 25, 1990Assignee: Sumitomo Chemical Company, LimitedInventors: Naoto Meki, Kazue Nishida, Tomotoshi Imahase, Hiroaki Fujimoto, Kenichi Mikitani, Hirotaka Takano, Yoriko Ogasawara, Masahiro Iamaki
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Patent number: 4977161Abstract: The present invention provides a compound of the formula: ##STR1## process for their production, pharmaceutical compositions containing them and their pharmaceutical uses, and intermediates useful for their production and processes for the production of such intermediates. The compounds are used as anti-hyperlipoproteinemic agents for example.Type: GrantFiled: November 13, 1989Date of Patent: December 11, 1990Assignee: Nissan Chemical Industries, Ltd.Inventors: Yoshihiro Fujikawa, Mikio Suzuki, Hiroshi Iwasaki, Mitsuaki Sakashita, Masaki Kitahara
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Patent number: 4975441Abstract: A composition suitable for topical application to mammalian skin or hair for inducing, maintaining or increasing hair growth comprises:(i) a chemical inhibitor of glycosidase activity chosen from lactams having the structure: ##STR1## where A.sup.1 and A.sup.6 are --H, --CH.sub.3, ##STR2## --CH.sub.2 OT or ##STR3## A.sup.1 and A.sup.6 being the same or different, and at least one of which being the group: ##STR4## in a lactam ring; and where Q is --OT', --NHT' or a lactam linkage to A.sup.1 or A.sup.6 ;the Q groups being the same or different, and at least one of which is involved in a lactam linkage;and where T is the same or different and is chosen from --H, --C.sub.p H.sub.2p+1 or a metal ion,T' is --H or --COC.sub.p H.sub.2p+1, andp is an integer of from 1 to 22;provided that:where any of the Q groups is --OT' or --NHT',then that group or groups can be of either stereochemical configuration with respect to the plane of the ring; and(ii) a cosmetically acceptable vehicle for the chemical inhibitor.Type: GrantFiled: March 22, 1989Date of Patent: December 4, 1990Assignee: Unilever Patent Holdings B.V.Inventor: Walter T. Gibson
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Patent number: 4948879Abstract: Monoazo compounds conforming to the general formula (1) shown and defined hereinafter have very good fiber-reactive dye properties and dye hydroxy- and/or carboxamido-containing material, in particular fiber material, such as wool and in particular cellulose fibers, in strong fast shades. ##STR1## where the symbols have the following meanings: D is a benzene or naphthalene ring or a heterocyclic radical,R.sup.1 and R.sup.Type: GrantFiled: November 17, 1988Date of Patent: August 14, 1990Assignee: Hoechst AktiengesellschaftInventors: Horst Tappe, Dieter Oehme, Werner H. Russ
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Patent number: 4931454Abstract: An azachroman derivative of the formula ##STR1## wherein Z is(a) --N.dbd.CH--CH.dbd.CH--,(b) --CH.dbd.N--CH.dbd.CH--,(c) --CH.dbd.CH--N.dbd.CH-- or(d) --CH.dbd.CH--CH.dbd.N--;R.sup.1 is A,R.sup.2 is H or A, orR.sup.1 and R.sup.2 together are alkylene with 3-6 C atoms;R.sup.3 is OH or OAc,R.sup.4 is H, orR.sup.3 and R.sup.4 together are a bond;R.sup.5 is 1H-2-pyridon-1-yl, 1H-6-pyridazinon-1-yl, 1H-2-pyrimidinon-1-yl, 1H-6-pyrimidinon-1-yl, 1H-2-pyrazinon-1-yl or 1H-2-thiopyridon-1-yl, or 1H-2-pyridon-1-yl, 1H-6-pyridazinon-1-yl, 1H-2-pyrimidinon-1-yl, 1H-6-pyrimidinon-1-yl, 1H-2-pyrazinon-1-yl or 1H-2-thiopyridon-1-yl mono- or disubstituted by A, F, Cl, Br, I, OH, OA, OAc, NO.sub.2, NH.sub.2, AcNH, HOOC or AOOC;A is C.sub.1-6 -alkyl andAc is C.sub.1-18 -alkanoyl or C.sub.7-11 -aroyl;or a pharmaceutically acceptable salt thereof is claimed. This compound exhibits vasodilatory and anti-hypertensive effects and is suitable for the treatment of alopecia.Type: GrantFiled: September 23, 1988Date of Patent: June 5, 1990Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Manfred Baumgarth, Rolf Gericke, Ingeborg Lues, Jacques De Peyer, Rolf Bergmann
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Patent number: 4921982Abstract: This invention provides bicyclic carboxylic esters and amides, their pharmaceutical formulations, and a method for their use in treating migraine, emesis, gastrointestinal disorders, schizophrenia, or anxiety in mammals.Type: GrantFiled: June 14, 1989Date of Patent: May 1, 1990Assignee: Eli Lilly and CompanyInventors: Marlene L. Cohen, William B. Lacefield, David W. Robertson
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Patent number: 4920226Abstract: There is provided novel (2-imidazolin-2-yl)thieno and furo compounds, and intermediate compounds for the preparation thereof, and a method for controlling a wide variety of annual and perennial plant species therewith.Type: GrantFiled: May 30, 1989Date of Patent: April 24, 1990Assignee: American CyanamidInventors: Marinus Los, David W. Ladner, Barrington Cross
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Patent number: 4910310Abstract: Novel intermediates and method for the chemical synthesis of N-substituted 1,5-dideoxy-1,5-imino-L-fucitol derivatives are provided. A preferred intermediate is 1,5-dideoxy-1,5-imino-3, 4-O-isopropylidene-L-fucitol which is used to prepare the HIV inhibitor 1,5-dideoxy-1,5-imino-[N-.omega.-methyl caproate]-L-fucitol. These compounds are prepared in a short synthesis from the known compound 2,3-O-isopropylidene-D-lyxono-1,4-lactone or in a multi-step synthesis from D-galactose.Type: GrantFiled: October 3, 1988Date of Patent: March 20, 1990Assignee: G. D. Searle & Co.Inventors: Arthur L. Campbell, James R. Behling, Kevin A. Babiak, John S. Ng, Richard A. Mueller, George W. J. Fleet
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Patent number: 4904665Abstract: A benzylaminoaryl-dihydropyridinelactone compound of the formula (I) ##STR1## in which R.sup.1 represents hydrogen, halogen, cyano, nitro, C.sub.6 -C.sub.12 -aryl, C.sub.1 -C.sub.8 -alkyl, C.sub.1 -C.sub.8 -alkoxy, C.sub.1 -C.sub.6 -alkylthio, trifluoromethyl, trifluoromethoxy, trifluoromethylthio, difluoromethoxy, di-C.sub.1 -C.sub.5 -alkylamino, C.sub.1 -C.sub.6 -alkoxycarboxyl or C.sub.1 -C.sub.6 -alkylsulphonyl,R.sup.2 represents hydrogen, or represents a straight-chain, branched or cyclic, saturated or unsaturated hydrocarbon radical having up to 10 carbon atoms which is optionally substituted by C.sub.1 -C.sub.6 -alkoxy, C.sub.1 -C.sub.6 -alkylthio, C.sub.1 -C.sub.6 -alkylsulphonyl, halogen, cyano, hydroxyl, pyridyl, thienyl, pyrimidyl, piperidinyl, phenyl or an amino group, where the amino group carries two identical or different substituents from the series comprising C.sub.1 -C.sub.5 -alkyl, phenyl or benzyl,R.sup.3 represents C.sub.1 -C.sub.Type: GrantFiled: February 18, 1988Date of Patent: February 27, 1990Assignee: Bayer AktiengesellschaftInventors: Siegfried Goldmann, Rainer Gross, Martin Bechem, Michael Kayser, Matthias Schramm, Siegbert Hebisch
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Patent number: 4904784Abstract: A compound of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein all the symbols are defined in the specification; having pharmacological activity, including blood pressure lowering activity, a process and intermediates for their preparation and their use as pharmaceuticals.Type: GrantFiled: February 23, 1989Date of Patent: February 27, 1990Assignee: Beecham Group p.l.c.Inventors: John M. Evans, Geoffrey Stemp, Frederick Cassidy
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Patent number: 4894378Abstract: Blood sugar levels are reduced by administration of novel 4-thienyl-dihydropyridines of the formula ##STR1## in which R.sup.1 represents 1 or 2 halogen atoms, or represents straight-chain, branched or cyclic alkyl with up to 8 carbon atoms,R.sup.2 represents a straight-chain, branched or cyclic, saturated or unsaturated hydrocarbon radical which has up to 15 carbon atoms, is optionally interrupted by one or two oxygen atoms, -N-phenyl or --SO.sub.n -- (n=0, 1 or 2) and is optionally substituted by halogen, phenyl, hydroxyl, cyano, amino, C.sub.1 -C.sub.6 -alkylamino, di-C.sub.1 -C.sub.6 -alkylamino, pyridyl, piperidino, N-phenylpiperazino, N-methylpiperazino, morpholino or N-benzyl-N-methyl-amino,R.sup.3 represents hydrogen, or represents straight-chain, branched or cyclic alkyl which has up to 6 carbon atoms and is optionally substituted by halogen, hydroxyl, amino or amino-C.sub.1 -C.sub.6 -alkoxy, or represents cyano or formyl andR.sup.Type: GrantFiled: June 22, 1988Date of Patent: January 16, 1990Assignee: Bayer AktiengesellschaftInventors: Siegfried Goldmann, Hilmar Bischoff, Walter Puls, Joachim Bender, Dieter Petzinna, Klaus Schlossmann
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Patent number: 4880924Abstract: This invention relates to a selective process for preparing bicyclic lactam-lactone compounds wherein the rings are fused, i.e. the rings share at least two carbon atoms, or are isolated. In particular, the present invention provides a process for selectively reacting novel 1-hydrocarbylamino (or heteroatom-substituted hydrocarbylamino); 1,1-dicarboxylic acid, alkylesters; 1-alkanolactonyl or hydrocarbyl (or heteroatom-substituted hydrocarbyl) alkanonylactonyl methane, as the salt of an acid having a pKa of 0 or more, to provide bicyclic lactam-lactone compounds. The selectively of the reaction to either fused or isolated bicyclic compounds is controlled by cyclizing the novel salts, in the absence of a base, a cyclizing said novel salts, in the presence of an amount of base substantially equivalent to said acid, respectively.Type: GrantFiled: April 3, 1986Date of Patent: November 14, 1989Assignee: Nelson Research & Development Co.Inventors: James V. Peck, Gevork Minaskanian
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Patent number: 4876357Abstract: Chromogenic phthalides and azaphthalides of the formula ##STR1## in which V.sub.1 and V.sub.2 are each, independently of the other, hydrogen, halogen, lower alkyl, lower alkoxy, (lower alkoxy)carbonyl or --NR.sub.1 R.sub.2, at least one of the radicals V.sub.1 and V.sub.2 being lower alkoxy or --NR.sub.1 R.sub.2, A is an unsubstituted or halogen-, cyano-, nitro-, (lower alkyl)-, (lower alkoxy)-, (lower alkyl)thio-, (lower alkyl)amino- or di(lower alkyl)amino-substituted benzene, naphthalene, pyridine, quinoline, pyrazine or quinoxaline ring, B is a substituted phenyl radical of the formula ##STR2## or a 3-indolyl of the formula ##STR3## Q is ##STR4## --S-- or --O--, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are each, independently of the others, hydrogen, unsubstituted or halogen-, hydroxy-, cyano- or (lower alkoxy)-substituted alkyl, cycloalkyl or unsubstituted or ringsubstituted phenalkyl or phenyl, or the substituent pairs (R.sub.1 and R.sub.2) and (R.sub.3 and R.sub.Type: GrantFiled: October 26, 1987Date of Patent: October 24, 1989Assignee: Ciba-Geigy CorporationInventors: Rox Phaff, Davor Bedekovic
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Patent number: 4866074Abstract: This invention relates to substituted pyridooxazinone and naphtheridone pyridones which are useful as cardiotonic agents for the treatment of congestive heart failure, to methods for increasing cardiac contractility using said compounds, and pharmaceutical compositions including the same.Type: GrantFiled: October 11, 1988Date of Patent: September 12, 1989Assignee: Rorer Pharmaceutical CorporationInventors: Alfred P. Spada, William L. Studt, Henry F. Campbell, Donald E. Kuhla, Thomas Tucker
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Patent number: 4847264Abstract: A class of bicyclic nitrogen heterocyclic ether and thioether compounds exhibiting pharmacological activity including cytoprotective, H.sub.2 -antagonist, anti-secretory and anti-ulcerogenic activity, pharmaceutical compositions comprising these compounds, and methods for the treatment of gastrointestinal hyperacidity and ulcerogenic disorders in mammals using said compositions are disclosed.Type: GrantFiled: December 23, 1986Date of Patent: July 11, 1989Assignee: Rorer Pharmaceutical CorporationInventors: Henry F. Campbell, Donald E. Kuhla, William L. Studt, Stuart A. Dodson
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Patent number: 4829066Abstract: This invention relates to substituted pyridooxazinone pyridazinone and pyrazolone compounds, which are useful as cardiotonic agents for the treatment of congestive heart failure. This invention also relates to methods for increasing cardiac contractility using said compounds, and pharmaceutical compositions including said compound.Type: GrantFiled: May 8, 1987Date of Patent: May 9, 1989Assignee: Rorer Pharmaceutical CorporationInventors: Alfred P. Spada, William L. Studt, Henry F. Campbell, Donald E. Kuhla
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Patent number: 4822794Abstract: This invention relates to substituted pyridooxazinone pyridones which are useful as cardiotonic agents for the treatment of congestive heart failure, to methods for increasing cardiac contractility using said compounds, and pharmaceutical compositions including the same.Type: GrantFiled: May 8, 1987Date of Patent: April 18, 1989Assignee: Rorer Pharmaceutical CorporationInventors: Alfred P. Spada, William L. Studt, Henry F. Campbell, Donald E. Kuhla
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Patent number: 4820840Abstract: An improved process for producing fluorene compounds of the following formula (II) is disclosed: ##STR1## (wherein R.sub.1, R.sub.2 and R.sub.3 are independently a hydrogen atom, an alkylamino group, a dialkylamino group, a pyrrolidino group or a piperdino group; X and Y are independently a carbon atom or a nitrogen atom; and with the proviso that R.sub.1 and R.sub.2 are not hydrogen atoms simultaneously). The process comprises reacting a lactone compound of the formula (I) (variables being defined as in formula (II) ) ##STR2## with a mixture of an aluminum halide, a carbonyl compound, and a hydroxy bearing compound.Type: GrantFiled: January 22, 1988Date of Patent: April 11, 1989Assignee: Appleton Papers Inc.Inventors: Seishi Ikegami, Satoshi Nakao
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Patent number: 4816588Abstract: The present invention provides a novel method for the preparation of pyridine-2,3-dicarboxylic acids by the oxidation of 8-substituted quinolines.Type: GrantFiled: August 19, 1987Date of Patent: March 28, 1989Assignee: American Cyanamid CompanyInventors: William F. Rieker, William A. Daniels
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Patent number: 4812459Abstract: A compound of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein all the symbols are defined in the specification; having pharmacological activity, including blood pressure lowering activity, a process and intermediates for their preparation and their use as pharmaceuticals.Type: GrantFiled: June 6, 1986Date of Patent: March 14, 1989Assignee: Beecham Group p.l.c.Inventors: John M. Evans, Geoffrey Stemp, Frederick Cassidy
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Patent number: 4808595Abstract: Furopyridine sulfonamides are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure and disorders associated therewith such as glaucoma.Type: GrantFiled: May 5, 1988Date of Patent: February 28, 1989Assignee: Merck & Co., Inc.Inventor: Jacob M. Hoffman, Jr.
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Patent number: 4806535Abstract: This invention relates to imidazolylphenyl and 1,2,4-triazolylphenyl benzopyridazinone and pyridopyridazinone compounds of the formula ##STR1## wherein A is CH or N and not more than one of W, X, Y and Z is a N atom which possess valuable pharmaceutical preparations, e.g., increasing cardiotonic contractility. Uses of said compounds including methods for increasing cardiac contractility and in the treatment of congestive heart failure, pharmaceutical compositions including the same and methods for the preparation thereof.Type: GrantFiled: July 22, 1987Date of Patent: February 21, 1989Assignee: Rorer Pharmaceutical CorporationInventors: William C. Faith, Henry F. Campbell, Donald E. Kuhla, William L. Studt, James L. Barnes
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Patent number: 4804667Abstract: 4 Aminoaryldihydropyridines of the formula ##STR1## in which R.sup.1 is hydrogen or an organic radical, preferably methyl or ethyl,R.sup.2 is hydrogen, C.sub.1 -C.sub.5 -alkyl, --CN, --NH.sub.2, --CH.sub.2 or --CH.sub.2 OH, preferably methyl,R.sup.3 is hydrogen or alkyl, preferably hydrogen,Y is --CO-- or --SO.sub.2 --, andR.sup.4 is an organic radical, orY--R.sup.4 is hydrogen,and physiologically acceptable salts thereof, are circulation-active and effective for improving myocardial contractility, for raising blood pressure, for lowering blood sugar, for reducing mucosal swelling and for controlling the salt and fluid balance.Type: GrantFiled: December 22, 1986Date of Patent: February 14, 1989Assignee: Bayer AktiengesellschaftInventors: Siegfried Goldmann, Matthias Schramm, Rainer Gross, Gunther Thomas, Martin Bechem, Michael Kayser
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Patent number: 4803275Abstract: The present invention relates to a compound FA-4283 or its derivative of the formula: ##STR1## wherein R is hydrogen or lower alkyl, and 3,4- and 3',4'-double bond may be saturated with hydrogens, and the method of production thereof.The compound (I) of the invention has an action of inhibiting fatty acid synthesis, thus being useful as an agent for prophylaxis and improvement of disorders of glucose and lipid methabolism.Type: GrantFiled: September 2, 1987Date of Patent: February 7, 1989Assignee: Takeda Chemical Industries, Ltd.Inventors: Tsuneo Kanamaru, Susumu Shinagawa, Masayuki Muroi
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Patent number: 4801715Abstract: Blood sugar levels are reduced by administration of novel 4-thienyl-dihydropyridines of the formula ##STR1## in which R.sup.1 represents 1 or 2 halogen atoms, or represents straight-chain, branched or cyclic alkyl with up to 8 carbon atoms,R.sup.2 represents a straight-chain, branched or cyclic, saturated or unsaturated hydrocarbon radical which has up to 15 carbon atoms, is optionally interrupted by one or two oxygen atoms, -N-phenyl or --SO.sub.n --(n=0, 1 or 2) and is optionally substituted by halogen, phenyl, hydroxyl, cyano, amino, C.sub.1 -C.sub.6 -alkylamino, di-C.sub.1 -C.sub.6 -alkylamino, pyridyl, piperidino, N-phenylpiperazino, N-methylpiperazino, morpholino or N-benzyl-N-benzyl-N-methyl-amino,R.sup.3 represents hydrogen, or represents straight-chain, branched or cyclic alkyl which has up to 6 carbon atoms and is optionally substituted by halogen, hydroxyl, amino or amino-C.sub.1 -C.sub.6 -alkoxy, or represents cyano or formyl andR.sup.Type: GrantFiled: December 4, 1986Date of Patent: January 31, 1989Assignee: Bayer AktiengesellschaftInventors: Siegfried Goldmann, Hilmar Bischoff, Walter Puls, Joachim Bender, Dieter Petzinna, Klaus Schlossmann
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Patent number: 4792606Abstract: A process for the preparation of a dimeric aromatic acyl cyanide of the formula ##STR1## in which Ar is optionally substituted phenyl, naphthyl or hetaryl,comprising reaction an acyl halide of the formulaAr--CO--Halin whichHal is fluorine, chlorine or bromine, with an alkali metal cyanide in a two-phase system comprising water and a water-immiscible or only sparingly water-miscible aliphatic ketone, and in the presence of a phase-transfer catalyst. The products are known intermediates for pesticides.Type: GrantFiled: July 16, 1987Date of Patent: December 20, 1988Assignee: Bayer AktiengesellschaftInventors: Reinhard Lantzsch, Hermann-Dieter Krall
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Patent number: 4786641Abstract: Blood-sugar-lowering dihydropyridines of the formula ##STR1## in which R.sup.1 represents phenyl, naphthyl, thienyl, pyridyl, chromenyl or thiochromenyl, it being possible for the radicals mentioned each to carry up to 2 identical or different substituents from the series comprising halogen, alkyl, alkoxy and alkylthio with in each case up to 6 carbon atoms, fluoroalkyl and fluoroalkoxy with in each case up to 3 carbon atoms and 3 fluorine atoms, nitro and cyano,R.sup.2 represents straight-chain, branched or cyclic alkyl which has up to 8 carbon atoms, can be interrupted in the alkyl chain by an oxygen or a sulphur atom and can be substituted by halogen, phenyl, cyano, hydroxyl, amino, alkylamino or dialkylamino with in each case up to 3 carbon atoms per alkyl group or by N-benzylmethylamino,R.sup.Type: GrantFiled: August 20, 1987Date of Patent: November 22, 1988Assignee: Bayer AktiengesellschaftInventors: Siegfried Goldmann, Hans-Jurgen Ahr, Walter Puls, Hilmar Bischoff, Dieter Petzinna, Klaus Schlossmann, Joachim Bender
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Patent number: 4778891Abstract: A pyranoindolizine derivative represented by the following general formula (I): ##STR1## wherein R means a hydrogen atom or hydroxyl group and Q denotes >C.dbd.O or ##STR2## with a proviso that Q is other than >C.dbd.O when R is a hydrogen atom. Its preparation process is also described.Type: GrantFiled: October 16, 1986Date of Patent: October 18, 1988Assignees: Daiichi Seiyaku Co., Ltd., Kabushiki Kaisha Yakult HonshaInventors: Hiroaki Tagawa, Hirofumi Terasawa, Akio Ejima
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Patent number: 4772611Abstract: Novel cardioactive compounds of the formula ##STR1## in which R.sup.1 is alkyl, aryl or heterocyclic, preferably substituted phenyl,R.sup.2 is alkyl, preferably methyl,R.sup.3 is hydrogen, halogen, acyloxy or alkyl, preferably hydrogen, andR.sup.4 is phenyl, carbalkoxy or together with R.sup.3 forms a ring, preferably carbalkoxy,are produced by reducing the corresponding nitro compounds.Type: GrantFiled: April 28, 1987Date of Patent: September 20, 1988Assignee: Bayer AktiengesellschaftInventors: Jurgen Stoltefuss, Fred R. Heiker, Martin Bechem, Rainer Gross, Michael Kayser, Matthias Schramm, Gunter Thomas