Polycyclo Ring System Having One Of The Two Rings Which Form The Spiro As One Of The Cyclos Patents (Class 548/411)
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Patent number: 5130442Abstract: Compounds of the formula ##STR1## in which R.sup.1 /R.sup.2 are alkyl, cycloalkyl, aralkyl or alkylene,R.sup.3 is alkyl, cycloalkyl or aralkyl,Z is alkylene,X is O orare highly suitable as color formers in recording materials based on acid developers. They give yellow or orange hues which have excellent sublimation and light fastness.Type: GrantFiled: October 31, 1990Date of Patent: July 14, 1992Assignee: Bayer AktiengesellschaftInventors: Karlheinrich Meisel, Hubertus Psaar
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Patent number: 5098925Abstract: The present invention relates to spiroisoindolines that are antagonists at the phencyclidine receptor of the N-methyl-D-aspartate receptor complex and which are useful when such antagonism is desired such as in the treatment of neurological disorders. The invention further provides processes for preparing the spiroisoindolines, intermediates useful for their synthesis, pharmaceutical compositions containing them, and methods for their use.Type: GrantFiled: February 5, 1991Date of Patent: March 24, 1992Assignee: ICI Americas Inc.Inventor: Thomas M. Bare
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Patent number: 5093500Abstract: A 1,6-diaza[4.4]spirodilactam monomer or oligomer having an aliphatically-unsaturated imido-containing substituent on each terminal spiro ring nitrogen atom and cured products thereof.Type: GrantFiled: October 17, 1990Date of Patent: March 3, 1992Assignee: Shell Oil CompanyInventor: Pen-Chung Wang
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Patent number: 5091387Abstract: Disclosed are spirocyclic compounds of the formula: ##STR1## The compounds of formula I are oxytocin antagonists useful in the treatment of preterm labor and dysmenorrhea, and for the stoppage of labor preporatory to Caesarian delivery. Also disclosed are pharmaceutical compositions containing these compounds as well as methods for preparing the compounds.Type: GrantFiled: August 5, 1991Date of Patent: February 25, 1992Assignee: Merck & Co., Inc.Inventors: Ben E. Evans, Douglas J. Pettibone, Roger M. Friedinger
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Patent number: 5076835Abstract: There are provided aryloxy-1'-(substituted)-spiro[cycloalkane-1,3'-indolin]-2'-one compounds, their herbicidal use, particularly for the selective control of undesirable plant species in the presence of cereal crops such as rice and wheat, and a method for the preparation thereof.Type: GrantFiled: May 31, 1990Date of Patent: December 31, 1991Assignee: America Cyanamid CompanyInventors: Michael E. Condon, Gary M. Karp, Jeffrey H. Birk
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Patent number: 5064852Abstract: A series of novel 3-mono(substituted methyl)- and 3,3-di(substituted methyl)-2-oxo-indoline-1-alkanoic acid compounds have been prepared, including their lower alkyl esters and unsubstituted amide derivatives, as well as the base salts of said acids with pharmacologically acceptable cations. These compounds are useful in therapy as aldose reductase inhibitors for the control of certain chronic diabetic complications. Typical members include those compounds derived from 2-oxo-indoline-1-acetic acid wherein a 3,4-dichlorobenzyl or 3,4-dichloro-.alpha.-methylbenzyl moiety is substituted at 3-position of the molecule. Preferred member compounds include 3-(3,4-dichlorobenzyl)-2-oxo-indoline-1-acetic acid, 5-chloro-3-(3,4-dichlorobenzyl)-2-oxo-indoline-1-acetic acid, 3-(3,4-dichlorobenzyl)-6-methoxy-2-oxo-indoline-1-acetic acid, 3-(3,4-dichlorobenzyl)-6-hydroxy-2-oxo-indoline-1-acetic acid and 3-(3,4-dichloro-.alpha.-methylbenzyl)-2-oxo-indoline-1-acetic acid.Type: GrantFiled: August 1, 1990Date of Patent: November 12, 1991Assignee: Pfizer Inc.Inventors: Harry R. Howard, Jr., Reinhard Sarges
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Patent number: 5043346Abstract: The invention relates to amino acid esters of the formula I ##STR1## in which n is 2 and R, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 have the meaning indicated in the description, to a process and intermediates for the preparation thereof, to agents containing them, and the use thereof.Type: GrantFiled: April 20, 1989Date of Patent: August 27, 1991Assignee: Hoechst AktiengesellschaftInventors: Franz Hock, Josef Scholtholt, Hansjorg Urbach, Rainer Henning, Ulrich Lerch, Wolf-Ulrich Nickel, Wolfgang Ruger
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Patent number: 5019587Abstract: The present invention provides compounds of the general formula (I) which inhibit the aggregation of erythrocytes or thrombocytes ##STR1## wherein A is hydrogen or C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl, C.sub.2 -C.sub.6 -alkynyl, benzyl or C.sub.3 -C.sub.7 -cycloalkyl radical, B is hydrogen, R.sub.1 is a C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl or C.sub.3 -C.sub.7 -cycloalkyl radical, R.sub.2 is a C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl, C.sub.3 -C.sub.7 -cycloalkyl, C.sub.1 -C.sub.6 -alkylcarbonyl, C.sub.1 -C.sub.6 -alkoxycarbonyl, aminocarbonyl or hydrazinocarbonyl radical, or R.sub.1 and R.sub.2, together with the carbon atom to which they are attached, form a C.sub.3 -C.sub.7 -cycloalkyl ring, n is 0, X is a valency bond or a C.sub.1 -C.sub.6 -alkylene radical, R.sub.3 is a carbocyclic aromatic ring, which may be substituted; and the tautomers, optically-active forms and physiologically acceptable salts thereof with organic and inorganic acids.Type: GrantFiled: June 5, 1989Date of Patent: May 28, 1991Assignee: Boehringer Mannheim GmbHInventors: Wolfgang V. Von Der Saal, Alfred Mertens, Erwin Boehm
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Patent number: 4985448Abstract: Lactam compounds of the formula ##STR1## in which: R is hydrogen, alkyl or cycloalkyl;R.sup.1 is hydrogen, alkyl, alkenyl or cycloalkyl;R.sup.2 is alkyl, alkenyl, cyano or a carbonyl substituted hydroxyl, alkyl, alkoxy, amino, alkylamino or hydrazino; orR.sup.1 and R.sup.2 together represent alkylidene cycloalkylidene; orR.sup.1, R.sup.2 and the adjacent carbon atom form a spirocyclic ring;n is 0 or 1;A is a --Co--NH--, --NH--CO--NH-- or --O--CO--NH--;X is a valency bond, alkylene or alkenylene; andR.sup.3 is optionally substituted phenyl, pyridyl, methylenedioxyphenyl or a five-membered heterocycle; or when X is a valency bond, R.sup.3 can also be an optionally substituted alkyl or alkino group, or cycloalkyl. The compounds are useful for the inhibition of erythrocyte and thrombocyte aggregation.Type: GrantFiled: February 6, 1989Date of Patent: January 15, 1991Assignee: Boehringer Mannheim GmbHInventors: Harald Zilch, Alfred Mertens, Wolfgang Von Der Saal, Erwin Boehm, Klaus Strein
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Patent number: 4983623Abstract: The invention relates to derivatives of cyclic amino acids of the general formula ##STR1## in which R.sup.1 denotes hydrogen, alkyl, alkenyl or (subst.) aryl,R.sup.2 is hydrogen, alkyl, hydroxyl, alkoxy, (subst.) aryl, (subst.) aryloxy or (subst.) aroyl, or R.sup.1 and R.sup.2 together represent (subst.) benzylidene, or R.sup.1 and R.sup.2, together with the carbon atom carrying them, represent (subst.) cycloalkyl, R.sup.3 denotes hydrogen, hydroxymethyl, formyl, (subst.) alkenyl, (subst.) carboxycarbonyl, (subst.) carbamoylcarbonyl or (subst.) trifluoromethylcarbonyl, A represents a cyclic amino acid, X denotes oxygen, imino or N-alkylimino, m is 0-5 and n is 0 or 1, to a process for the preparation thereof, to agents containing them, and to the use thereof.Type: GrantFiled: December 13, 1988Date of Patent: January 8, 1991Assignee: Hoechst AktiengesellschaftInventors: Rainer Henning, Hansjorg Urbach, Franz Hock
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Patent number: 4963686Abstract: The new pyrrolobenzimidazoles according to the present invention are compounds of the general formula: ##STR1## wherein R.sub.1 is a hydrogen atom or an alkyl, alkenyl or cycloalkyl radical, R.sub.2 is a hydrogen atom, an alkyl or alkenyl radical or a cyano group or a carbonyl group substituted by a hydroxyl or hydrazino group or by an alkyl, alkoxy, amino, alkylamino or dialkylamino group or together with R.sub.1 represents a cycloalkylene radical or R.sub.1 and R.sub.2 together form an alkylidene or cycloalkylidene radical, X is a valency bond, a C.sub.1 -C.sub.4 alkylene radical or a vinylene radical, T is an oxygen or sulphur atom and Py is a 2-, 3- or 4-pyridyl radical which optionally carries an oxygen atom on the ring heteroatom and/or can be substituted one or more times by alkyl, alkoxy, hydroxyl, cyano or nitro, as well as by halogen; the tautomers thereof and the physiologically acceptable salts thereof with inorganic and organic acids.Type: GrantFiled: July 5, 1988Date of Patent: October 16, 1990Assignee: Boehringer Mannheim GmbHInventors: Jens-Peter Holck, Alfred Mertens, Wolfgang Kampe, Bernd Muller-Beckmann, Gisbert Sponer, Klaus Strein
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Patent number: 4940703Abstract: The present invention provides a compound of formula I or a salt or prodrug thereof: ##STR1## wherein the dotted line represents an optional chemical bond in one of the two possible positions;A represents a group of formula II: ##STR2## in which R.sup.1 represents hydrogen, hydroxy, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.1-6 alkoxy, benzyloxy, hydroxy (C.sub.1-6)alkyl, halogen, amino, cyano, nitro, --CONR.sup.6 R.sup.7 or --SO.sub.2 NR.sup.6 R.sup.7, in which R.sup.6 and R.sup.7 independently represent hydrogen, halogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl or C.sub.2-6 alkynyl;R.sup.2 represents hydrogen, halogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or C.sub.1-6 alkylcarbonyl;V represents nitrogen, --CH or --C--; andW represents oxygen, sulphur or --NR.sup.8, in which R.sup.8 represents hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl or C.sub.Type: GrantFiled: April 4, 1989Date of Patent: July 10, 1990Assignee: Merck Sharp & Dohme LimitedInventors: Raymond Baker, Clare O. Kneen, John Saunders, Christopher Swain
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Patent number: 4939270Abstract: Primary diamines, employed in stoichiometric excess, react with a spirodilactam precursor selected from 4-oxoheptandioic acid compounds or 1,6-dioxaspiro[4.4]nonane-2,7-diones, to produce 1,6-diaza[4.4]spirodilactams having an amino-containing substituent on each spiro ring nitrogen atom. The spirodilactams are useful in the production of thermoplastic polyamides by reaction with diacids and as curing agents for epoxy resins in the production of thermoset resins.Type: GrantFiled: February 23, 1989Date of Patent: July 3, 1990Assignee: Shell Oil CompanyInventor: Pen C. Wang
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Patent number: 4933336Abstract: A compound of formula (I), or a pharmaceutically acceptable salt thereof, ##STR1## in which, R.sub.1 is hydrogen, lower alkyl or CH.sub.2 OR.sub.6 ;R.sub.2 is hydrogen or lower alkyl;R.sub.3 is hydrogen or lower alkyl;each of W and Z, which are different, represents --CR.sub.4 R.sub.5 -- or --(CR.sub.x R.sub.y).sub.n --, in which,R.sub.4 is hydrogen, C.sub.1-3 alkyl, C.sub.1-3 alkylthio or C.sub.1-3 alkoxy;R.sub.5 is C.sub.1-3 alkyl, C.sub.1-3 alkylthio or C.sub.1-3 alkoxy; or together R.sub.4 and R.sub.5 form a 3 to 6 membered carbocyclic ring, or a heterocyclic ring containing one or two ring oxygen, nitrogen or sulphur atoms;or R.sub.4 and R.sub.5 together form an oxo or methylene group;each of R.sub.x and R.sub.y is hydrogen or C.sub.1-3 alkyl; n is zero or 1;R.sub.6 is hydrogen, lower alkyl, lower alkylcarbonyl, arylcarbonyl, aralkylcarbonyl, heteroarylcarbonyl, optionally substituted aminocarbonyl, lower alkoxycarbonyl and aryloxycarbonyl;R.sub.Type: GrantFiled: August 9, 1988Date of Patent: June 12, 1990Assignee: Laboratoires Sobio S.A.Inventors: Michel Martin, Guy Nadler, Richard Zimmermann
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Patent number: 4927917Abstract: There are provided compounds which give quasi-liquid crystals, which comprise a mesogenic group, which can contain bridging groups, a bridging group and a spiropyran moiety having a 2H pyran ring, a terminal group being attached to the mesogenic group. The mesogenic group contains two aromatic, heterocyclic or cycloaliphatic ring structures. The compounds are prepared by a coupling reaction of mesogenic groups with a spiropyran compound via a suitable bridging group. There is provided a process for producing quasi-liquid crystalline (QLC) films which are useful for producing a wide variety of devices based on the optical non-linearity of generation of second harmonics by such films. Such devices can also be based on ferroelectric, pyroelectric, piezoelectric effects and photoactivity of such oriented QLC films.Type: GrantFiled: December 19, 1988Date of Patent: May 22, 1990Assignee: Yeda Research and Development Co., Ltd.Inventors: Valeri A. Krongauz, Felix P. Shvartsman
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Patent number: 4925841Abstract: Mannich bases of spirosuccinimides are provided having anticonvulsant, sedative and antileukemic activity.Type: GrantFiled: June 27, 1988Date of Patent: May 15, 1990Assignee: Temple University of the Commonwealth System of Higher EducationInventors: Michael R. Borenstein, Peter H. Doukas
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Patent number: 4920127Abstract: Compounds of formula (I), or a pharmaceutically acceptable salt thereof: ##STR1## wherein L is NH or O;R.sub.1 is hydrogen, fluoro or chloro;R.sub.2 and R.sub.5 are independently hydrogen or C.sub.1-6 alkyl or together are a bond; orR.sub.2 and R.sub.3 and/or R.sub.4 and R.sub.5, together are C.sub.2-7 polymethylene or --(CH.sub.2).sub.m --O--(CH.sub.2).sub.x -- where m and x. are 1 to 5 such that m+x is 2 to 6;R.sub.4 is C.sub.1-7 acyl, C.sub.1-6 alkoxycarbonyl, hydroxycarbonyl, aminocarbonyl optionally substituted by one or two C.sub.1-6 alkyl groups, CF.sub.3, C.sub.1-6 alkyl substituted by C.sub.1-6 alkoxy, C.sub.1-6 alkylthio or by C.sub.1-6 alkoxycarbonyl, or R.sub.4 is phenyl or phenyl-C.sub.1-4 alkyl optionally substituted in the phenyl ring by one or two of halogen, C.sub.1-6 alkyl or C.sub.1-6 alkoxy;Z is a group of formula (a), (b) or (c).Type: GrantFiled: February 16, 1988Date of Patent: April 24, 1990Assignee: Beecham Group p.l.c.Inventors: Francis D. King, Karen A. Joiner
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Patent number: 4877785Abstract: Non-peptidyl compounds characterized generally as .beta.-succinamidoacyl aminodios are useful as renin inhibitors for the treatment of hypertension.Type: GrantFiled: October 1, 1987Date of Patent: October 31, 1989Assignee: G. D. Searle & Co.Inventors: Gunnar J. Hanson, John S. Baran
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Patent number: 4874756Abstract: The present invention provides compounds of the general formula ##STR1## wherein the variables are as defined herein. The present invention also provides processes for the preparation thereof, pharmaceutical compositions containing them and intermediates for the preparation thereof.Type: GrantFiled: August 29, 1986Date of Patent: October 17, 1989Assignee: Boehringer Mannheim GmbHInventors: Alfred Mertens, Wolfgang von der Saal, Herbert Berger, Bernd Muller-Beckmann, Klaus Strein
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Patent number: 4871656Abstract: A dye useful for absorbing infrared radiation in photographic elements, having the structure: ##STR1## is disclosed. In this formula, R.sub.1 and R.sub.2 each independently represents sulfoalkyl, carboxyalkyl, or sulfatoalkyl, from 2 to 4 carbon atoms, having 2 carbon atoms in the alkyl chain linking the nitrogen atom of each Z ring and the sulfo or sulfato group, and 1 carbon atom in the alkyl chain linking the nitrogen atom of each Z ring and the carboxy group.R.sub.3 and R.sub.5 are each hydrogen or together represent the atoms necessary to complete a 5- or 6-membered carbocyclic ring, and R.sub.4 represents hydrogen, alkyl of 1 to 4 carbon atoms, halogen, cyano, or ##STR2## where R.sub.6 and R.sub.7 each independently represents alkyl of from 1 to 6 carbon atoms or aryl or together represent the non-metallic atoms necessary to form a 5- or 6-membered heterocyclic ring.X.sup..sym. represents a cation.Z.sub.1 and Z.sub.Type: GrantFiled: March 10, 1988Date of Patent: October 3, 1989Assignee: Eastman Kodak CompanyInventors: Richard L. Parton, ANthony D. Gingello, David J. Collett, David A. Stegman, ANthony Adin
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Patent number: 4864028Abstract: Disclosed are substituted or unsubstituted planar tricyclic fluorene or nuclear analogs thereof, spiro-coupled to a five-membered ring containing a secondary amide, and the pharmaceutically acceptable salts thereof. These compounds are useful, inter alia, in the treatment of diabetes. Also disclosed are processes for the preparation of such compounds; pharmaceutical compositions comprising such compounds; and methods of treatment comprising administering such compounds and compositions when indicated for, inter alia, long term, prophylactic treatment of the diabetes syndrome.Type: GrantFiled: September 9, 1987Date of Patent: September 5, 1989Assignee: Alcon Laboratories, Inc.Inventor: Billie M. York, Jr.
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Patent number: 4849524Abstract: The invention relates to a process for preparing compounds of the formula I ##STR1## in which R stands for hydrogen, alkyl or aralkyl and R.sup.1 to R.sup.5 are identical or different radicals, (substituted) alkyl, cycloalkyl or (substituted) aryl or in which the pairs of radicals R.sup.1 and R.sup.2, R.sup.2 and R.sup.3, and R.sup.4 and R.sup.5 together with the carbon atom(s) supporting them form a mono- or bicyclic ring system and the other radicals are hydrogen, by treating a compound of the formula II ##STR2## in which R and R.sup.1 and R.sup.5 have the abovementioned meaning and R.sup.6 and R.sup.7 denote alkyl or aralkyl or together with the nitrogen atom supporting them form a heterocycle which can additionally contain an oxygen atom, with a reducing agent.Type: GrantFiled: November 19, 1987Date of Patent: July 18, 1989Assignee: Hoechst AktiengesellschaftInventors: Rainer Henning, Hansjorg Urbach
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Patent number: 4826847Abstract: The present invention provides oxindole derivatives of the formula: ##STR1## wherein the various substituents are defined hereinbelow. The above compounds display nitrate-like as well as .beta.-blocking actions.Type: GrantFiled: December 30, 1986Date of Patent: May 2, 1989Assignee: Boehringer Mannheim GmbHInventors: Helmut Michel, Wolfgang Kampe, Klaus Strein, Wolfgang Bartsch
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Patent number: 4812567Abstract: There are disclosed compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 taken together represent ##STR2## with the proviso that in ##STR3## when X is lower alkylene or O, m is other than 1; and when R.sup.1 and R.sup.2 taken together represent ##STR4## R.sup.3 is other than unsubstituted or substituted 2-pyridinyl or 2-pyrimidinyl;R.sup.3 is unsubstituted or substituted 2-pyridinyl, 2-pyrimidinyl, 2-pyrazinyl or 3-pyridazinyl, where the substituents are selected from the group lower alkyl, lower alkoxy, halo, cyano and nitro;Z is --(CH.sub.2).sub.n -- or vinylene;X is lower alkylene, vinylene or O;m is 1-4;n is 1-3;o is 1-5;p is 0-1;and the pharmaceutically acceptable salts thereof and their use as antipsychotic/anxiolytic agents having a low liability for extrapyramidal side effects.Type: GrantFiled: December 17, 1986Date of Patent: March 14, 1989Assignee: American Home Products CorporationInventor: Magid A. Abou-Gharbia
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Patent number: 4810801Abstract: The present invention provides new pyrrolobenzimidazoles of the general formula: ##STR1## wherein R.sub.1 -R.sub.5, X and T are as defined in the specification. The present invention also provides processes for the preparation of these compounds and pharmaceuticals containing them for the prophylaxis and treatment of heart and circulatory diseases.Type: GrantFiled: October 1, 1987Date of Patent: March 7, 1989Assignee: Boehringer Mannheim GmbHInventors: Alfred Mertens, Jens-Peter Holck, Wolfgang Kampe, Bernd Muller-Beckmann, Klaus Strein, Wolfgang Schaumann
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Patent number: 4803217Abstract: Hapalindolinone compounds are produced by the controlled aerobic fermentation of a cyanobacterium of the genus Fischerella, ATCC No. 53558.Type: GrantFiled: December 24, 1986Date of Patent: February 7, 1989Assignee: Merck & Co., Inc.Inventors: Robert E. Schwartz, Charles F. Hirsch, Janet M. Sigmund, Douglas J. Pettibone
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Patent number: 4801721Abstract: Methods for the alkylation of substituted amines with trifluorate esters is disclosed.Type: GrantFiled: December 19, 1986Date of Patent: January 31, 1989Inventors: James W. Ryan, Alfred Chung
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Patent number: 4772722Abstract: Disclosed are nadimido-substituted cyclophosphazene derivatives and thermosets thereof. The thermosets are useful as high temperature, flame resistant matrices for composites and as metal adhesives.Type: GrantFiled: September 10, 1986Date of Patent: September 20, 1988Assignee: Hercules IncorporatedInventor: Alexander Lukacs, III
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Patent number: 4766141Abstract: Spiro-succinimides are disclosed which are useful as aldose reductase inhibitors and as therapeutic agents for the treatment of complications arising from diabetes. Pharmaceutical compositions containing the spiro- compounds and a method of treating diabetic complications are also disclosed.Type: GrantFiled: October 14, 1987Date of Patent: August 23, 1988Assignee: Pfizer Inc.Inventor: Christopher A. Lipinski
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Patent number: 4739074Abstract: Adamantane spiro-pyrrolidine derivatives, more specifically, spiro[pyrrolidine-5,2'-tricyclo[3.3.1.1.sup.3,7 ]decane]derivatives of the structure ##STR1## where X is oxygen or two hydrogen radicals and R is hydrogen or ##STR2## where R.sup.1 is a C.sub.1 -C.sub.18 alkyl radical, phenyl or phenylcyclopropyl, are disclosed herein. Said derivatives have been found to have activity in laboratory animal models against carrageenan-induced edema.Type: GrantFiled: January 22, 1986Date of Patent: April 19, 1988Assignee: Pennwalt CorporationInventors: Vassil S. Georgiev, George B. Mullen
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Patent number: 4622336Abstract: 3,3-Dialkyl- or 3,3-alkylene-indolines which are unsubstituted at the 1- and 2-positions and which are substituted at the 4- or 6-position by an optionally etherified hydroxy group or substituted at the 5- or 7-position by an etherified hydroxy group, as well as their physiologically-hydrolyzable and -acceptable esters. The said indolines and esters as well as their pharmaceutically acceptable acid addition salts possess analgesic activity.Type: GrantFiled: January 17, 1985Date of Patent: November 11, 1986Assignee: Sandoz Ltd.Inventor: Roland Achini
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Patent number: 4620012Abstract: The invention relates to new spirocyclic aminoacid derivatives of the formula I ##STR1## in which m denotes 1 or 2, n denotes 0 or 1, R denotes hydrogen, alkyl or aralkyl, R.sup.1 denotes hydrogen or alkyl which can be optionally substituted by amino, acylamino or benzoylamino, alkenyl, cycloalkyl, cycloalkenyl, cycloalkylalkyl, aryl or partially hydrogenated aryl, each of which can be substituted by alkyl, alkoxy or halogen, arylalkyl or aroylalkyl, both of which can be substituted as defined above in the aryl radical, an S- or O- and/or N-heterocyclic radical or a side chain of an .alpha.-aminoacid, R.sup.Type: GrantFiled: January 10, 1984Date of Patent: October 28, 1986Assignee: Hoechst AktiengesellschaftInventors: Rainer Henning, Hansjorg Urbach, Volker Teetz, Reinhard Becker
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Patent number: 4600776Abstract: Cationic enamine dyestuffs of the general formula ##STR1## in which the symbols have the meaning given in the description, are used for dyeing natural and synthetic substrates and compositions which can be dyed with cationic dyestuffs, in particular paper.Type: GrantFiled: June 11, 1984Date of Patent: July 15, 1986Assignee: Bayer AktiengesellschaftInventors: Karlheinrich Meisel, Roderich Raue
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Patent number: 4537892Abstract: Disclosed are substituted or unsubstituted planar tricyclic fluorene or nuclear analogs thereof, spiro-coupled to a five-membered ring containing a secondary amide, and the pharmaceutically acceptable salts thereof. These compounds are useful, inter alia, in the treatment of diabetes. Also disclosed are processes for the preparation of such compounds; pharmaceutical compositions comprising such compounds; and methods of treatment comprising administering such compounds and compositions when indicated for, inter alia, long term, prophylactic treatment of the diabetes syndrome.Type: GrantFiled: September 14, 1983Date of Patent: August 27, 1985Assignee: Alcon Laboratories, Inc.Inventor: Billie M. York, Jr.
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Patent number: 4524206Abstract: Disubstituted N,N'-piperazinyl derivatives are disclosed wherein one substituent is heteroaryl and the other is alkylene attached to the ring nitrogen of substituted 2,5-pyrrolidinedion-1-yl moieties. The substitution pattern of the pyrrolidinedione ring involves either geminal disubstitution, including spiro ring fusion, or 3,4-phenyl ring fusion to give phthalimide derivatives. Heteroaryl substitution on the other piperazine nitrogen comprises pyridine, pyrimidine, and benzisothiazole ring systems. Representative examples of these compounds demonstrate useful central nervous system effects.Type: GrantFiled: September 12, 1983Date of Patent: June 18, 1985Assignee: Mead Johnson & CompanyInventors: James S. New, Joseph P. Yevich
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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: 4452802Abstract: There are described antihypertensive spiro[benzofuran-azalkanes] of the formula ##STR1## where X is hydrogen or halogen (F, Cl, Br, or I); m and n are each 0, 1 or 2 but m plus n is 1 or 2; and R is ##STR2## k being 2 or 3 and Y being hydrogen or halogen, which are useful as antihypertensive agents and methods for synthesizing the same.Type: GrantFiled: August 25, 1983Date of Patent: June 5, 1984Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: Raymond W. Kosley, Jr., Robert J. Cherill
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Patent number: 4442114Abstract: A series of spiro-imide compounds and their base salts with pharmacologically acceptable cations are disclosed. These particular compounds are useful in therapy as agents for the control of certain chronic diabetic complications. Preferred member compounds include 2,3-dihydro-spiro-[1H-indene-1,3'-pyrrolidone]-2',5'-dione, 2,3-dihydro-spiro-[1H-indene-2,3'-pyrrolidine]-2',5'-dione, 3,4-dihydro-spiro-[2H-naphthalene-1,3'-pyrrolidine]-2',5'-dione, 3,4-dihydro-spiro-[2H-naphthalene-1,3'-piperidine]-2',6'-dione, 6-chloro-2,3-dihydro-spiro-[4H-1-benzopyran-4,3'-pyrrolidine]-2',5'-dione and 6,7-dihydro-spiro-[5H-benzo(b)thiophene-4,3'-pyrrolidine]-2',5'-dione. Methods for preparing these compounds from known starting materials are provided.Type: GrantFiled: January 17, 1983Date of Patent: April 10, 1984Assignee: Pfizer Inc.Inventors: John L. Belletire, Reinhard Sarges
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Patent number: 4431661Abstract: Novel compounds are disclosed having the formula ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are each individually selected from the class consisting essentially of hydrogen, hydroxy, chloro, bromo, an alkyl radical having up to 3 carbon atoms, an alkoxy radical having up to 3 carbon atoms, and trifluoromethyl, and any two or more of R.sub.1, R.sub.2 and R.sub.3 may be the same; R.sub.4 is selected from the class consisting essentially of hydrogen, an alkyl radical having up to 3 carbon atoms, an allyl radical having up to 4 carbon atoms, the cyclopropylmethyl radical or the phenethyl radical; and W and W' each represent a monovalent alkyl moiety having up to 3 carbon atoms or W-W' jointly represent a divalent moiety of the formula ##STR2## where n is an integer of 2 or 3, including individual optically active isomers, racemic mixtures thereof, and non-toxic pharmacologically-acceptable acid-addition salts thereof. Such compounds are useful as analgesics in mammals.Type: GrantFiled: August 20, 1981Date of Patent: February 14, 1984Assignee: American Cyanamid CompanyInventors: Thomas C. McKenzie, Joseph W. Epstein, William J. Fanshawe
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Patent number: 4408050Abstract: Novel spiro[indoline-3,4'-piperidine]s and related compounds and methods of preparing same are described. These compounds are useful as antidepressants, anticonvulsants and tranquilizers. Also described is a novel method of preparing indoline rings.Type: GrantFiled: December 18, 1981Date of Patent: October 4, 1983Assignee: American Hoechst CorporationInventors: Helen H. Ong, James A. Profitt
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Patent number: 4395416Abstract: Derivatives of formula: ##STR1## in which Z< represents: either an amino group of struture >N-R.sub.1 where R.sub.1 represents a linear or branched alkyl group with 1 to 5 carbon atoms or a phenyl group possibly substituted by a chlorine atom, in which case:n=1 or 2,the pair (A, C X) assumes the following values: (S, C.dbd.O), (S, CH.sub.2), (O, CH.sub.2), (O, CH--C.sub.6 H.sub.5), andR represents a hydrogen or halogen atom, one or more methoxy groups or the butadiene-1,3 ylene chain ##STR2## fixed in position 5,6 of the phenyhl nucleus and thus forming with this latter a naphthyl nucleus;or a methylene group (--CH.sub.2 --), in which case:n=1 or 2,A represents the oxygen atom,>C X represents a carbonyl group (>C.dbd.O) or thiocarbonyl group (>C.dbd.S), andR has the same meanings as previously,as well as the mineral or organic acid addition salts thereof. The compounds exhibit anti-convulsion and analgesic activity.Type: GrantFiled: January 21, 1982Date of Patent: July 26, 1983Assignee: Delalande S.A.Inventors: Michel Langlois, Bernard P. Bucher, Philippe L. Dostert, Alain P. Lacour, Gerard H. Moinet