Polycyclo Ring System Having The Six-membered Hetero Ring As One Of The Cyclos Patents (Class 546/18)
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Patent number: 4771091Abstract: Novel diazaspirodecanes of the general formula ##STR1## are prepared from known diazaspirodecane compounds and epoxy compounds or by reacting diazaspirodecane-substituted epoxy compounds with alcohols or amines and are excellent light stabilizers for synthetic polymers.Type: GrantFiled: November 24, 1986Date of Patent: September 13, 1988Assignee: Hoechst AktiengesellschaftInventor: Josef Ertl
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Patent number: 4731366Abstract: This invention relates to novel discorhabdin compositions which are useful as antitumor, antibacterial and antifungal compositions, a process of producing the compositions and a method for inhibiting tumors, bacteria and fungi utilizing the compositions. More particularly, the novel discorhabdin compositions are organic compounds which are derived from marine sponges genus Latrunculia.Type: GrantFiled: August 5, 1986Date of Patent: March 15, 1988Assignee: Harbor Branch Oceanographic Institution, Inc.Inventors: Murray H. G. Munro, Nigel B. Perry, John W. Blunt
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Patent number: 4717724Abstract: New 1-(1,3-dioxolan-2-ylmethyl)azoles, their stereoisomers and their salts are described, as are processes for their preparation. The new compounds are chemotherapeutic agents. They are active against skin fungi, mold fungi and yeasts and against bacteria.Type: GrantFiled: March 8, 1984Date of Patent: January 5, 1988Assignee: Hoechst AktiengesellschaftInventors: Wolfgang Schaper, Ernst Blume, Wolfgang Raether, Walter Dittmar
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Anti-depressant spiro hexahydro arylquinolizine derivatives, composition, and method of use therefor
Patent number: 4710504Abstract: Substituted hexahydro arylquinolizines and pharmaceutically acceptable salts thereof are selective .alpha..sub.2 -adrenergic receptor antagonists and thereby useful as antidepressants, antihypertensives, ocular antihypertensives, antidiabetics, platelet aggregation inhibitors, antiobesity agents, and modifiers of gastrointestinal motility.Type: GrantFiled: April 4, 1986Date of Patent: December 1, 1987Assignee: Merck & Co., Inc.Inventors: John J. Baldwin, Joel R. Huff, Joseph P. Vacca, Steven D. Young, Jane deSolms, James P. Guare, Jr. -
Patent number: 4652564Abstract: Substituted spiro pyridine derivatives are anti-allergic and anti-inflammatory agents. They are also useful for the treatment of peptic ulcers.Methods for their preparation and use are disclosed.Type: GrantFiled: December 14, 1983Date of Patent: March 24, 1987Assignee: Schering CorporationInventor: David J. Blythin
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Patent number: 4623380Abstract: Compounds of the formula ##STR1## in which A denotes C-R.sup.4 or N; X denotes alkyl and Y denotes alkyl, cycloalkyl, alkenyl, alkynyl, phenyl or benzoyl, or, together with X, cycloalkyl; R.sup.1 -R.sup.4 denote H, alkyl, alkoxy, alkoxycarbonyl, halogen, NO.sub.2, CN, phenoxy or (substituted) phenyl; R.sup.5 denotes H or alkyl; and R.sup.6 denotes H, (substituted) alkyl, halogenoalkenyl, cycloalk(en)yl, alkynyl, (substituted) phenyl or carboxylic acid ester, carboxylic acid amide, sulfo-ester or acyl radicals, are effective plant treatment agents, in particular herbicides.Type: GrantFiled: February 1, 1985Date of Patent: November 18, 1986Assignee: Hoechst AktiengesellschaftInventors: Roland Schmierer, Reinhard Handte, Hilmar Mildenberger, Klaus Bauer, Hermann Bieringer, Helmut Burstell
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Patent number: 4617305Abstract: The present invention is concerned with derivatives of 2,3,3a,4,5,6-hexahydro-1H-indolo(3,2,1-de)(1,5)naphthyridine of the formula ##STR1## in the form of base or acid addition salts, preferably with pharmaceutically acceptable acids, wherein one of the groups R1 and R2 represents a lower alkyl group and the other represents a hydrogen atom or R1 and R2 represent each independently an alkyl group or, together an alkanediyl group having from 4 to 6 carbon atoms. R3 represents a lower alkyl group, a hydrogen atom or a benzyl group. And either R5 represents a lower carboalkoxy group or a hydrogen atom and R6 represents with R4 an additional carbon-carbon bond; or R4 represents a hydrogen atom and R6 and R5 represent together an oxygen atom or respectively a hydrogen atom and a hydroxyl group.Type: GrantFiled: February 22, 1984Date of Patent: October 14, 1986Assignee: Omnichem, S.A.Inventor: Jean A. A. J. Hannart
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Patent number: 4617302Abstract: This invention provides certain pyridazinone derivatives, their pharmaceutical formulations, and their use as positive inotropic agents.Type: GrantFiled: October 15, 1984Date of Patent: October 14, 1986Assignee: Eli Lilly and CompanyInventor: David W. Robertson
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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: 4595754Abstract: A process for preparing a cis N-alkylperhydroquinoline comprising reacting a 3-chloropropyl N-alkylimine with a hydride reducing agent in a basic reaction medium at a temperature in the range of from about -20.degree. C. to about 25.degree. C.Type: GrantFiled: March 4, 1985Date of Patent: June 17, 1986Assignee: Eli Lilly and CompanyInventors: Randall K. Atkins, Leland O. Weigel
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Patent number: 4575507Abstract: Compounds related to 3',4'-dihydrospiro[imidazolidine-4,1'(2'H)-naphthalene]2,3',5-trione, spiro[chroman-4,4'-imidazolidine]2,2',5'-trione and 1',2'-dihydrospiro[imidazolidine-4,4'-(3'H)-quinoline 2,2'5-trione and reduced products thereof as aldose reductase inhibitors.Type: GrantFiled: May 29, 1985Date of Patent: March 11, 1986Assignee: Pfizer Inc.Inventor: Christopher A. Lipinski
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Patent number: 4556712Abstract: In a short total synthesis of morphinan compounds, derivatives of 1-benzyl-1,2,3,4-tetrahydroisoquinoline are produced. Certain of these compounds, although highly aromatic and functionalized, can be optically resolved. The optically active enantiomers can serve as important intermediates for both natural and unnatural opioids.Type: GrantFiled: March 18, 1983Date of Patent: December 3, 1985Assignee: The United States of America as represented by the Secretary of the Department of Health and Human ServicesInventor: Kenner C. Rice
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Patent number: 4550112Abstract: Novel 3,7-diaza bicyclo-(3,3,1)-nonane compounds are described which are represented by the formula: ##STR1## wherein Z.sub.1 and Z.sub.2 each denotes hydrogen,R.sub.1 and R.sub.2 each denotes (A) a substituent which contains up to 12 carbon atoms and which is selected from the group consisting of alkyl, alkenyl, and alkinyl, or (B) a cycloalkyl group containing 3 to 6 carbon atoms which is attached to the nitrogen atom directly or by an alkylene group containing 1 to 3 carbon atoms, andR.sub.3 and R.sub.4 each denotes an alkyl group with up to 7 carbon atoms, or both together form an alkylene chain represented by the formula --(CH.sub.2).sub.n --, wherein n is an integer ranging between about 3 and 6, such that the substituents R.sub.1, R.sub.2, R.sub.3, and R.sub.4 together contain at least 5 carbon atoms. Also described are processes of producing said compounds, pharmaceutical compositions containing compounds of Formula I, and methods of preparing and using said compositions.Type: GrantFiled: September 16, 1983Date of Patent: October 29, 1985Assignee: Kali-Chemie Pharma GmbHInventors: Uwe Schoen, Bernd Hachmeister, Wolfgang Kehrbach, Ulrich Kuehl, Gerd Buschmann
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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: 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: 4410700Abstract: In a short total synthesis of morphinan compounds, derivatives of 1-benzyl-1,2,3,4-tetrahydroisoquinoline are produced. Certain of these compounds, although highly aromatic and functionalized, can be optically resolved. The optically active enantiomers can serve as important intermediates for both natural and unnatural opioids.Type: GrantFiled: May 20, 1981Date of Patent: October 18, 1983Assignee: The United States of America as represented by the Department of Health and Human ServicesInventor: Kenner C. Rice
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Patent number: 4410699Abstract: Novel spiro[benzofuranisoquinoline]s, intermediates and processes for the preparation thereof and methods for alleviating pain, inhibiting convulsions, reducing blood pressure and producing diuresis employing the compounds or compositions thereof are disclosed.Type: GrantFiled: November 29, 1982Date of Patent: October 18, 1983Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Richard C. Effland, Larry Davis, Joseph T. Klein
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Patent number: 4374137Abstract: Novel spiro[benzofuranisoquinoline]s, intermediates and processes for the preparation thereof and methods for alleviating pain, inhibiting convulsions, reducing blood pressure and producing diuresis employing the compounds or compositions thereof are disclosed.Type: GrantFiled: August 7, 1981Date of Patent: February 15, 1983Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Richard C. Effland, Larry Davis, Joseph T. Klein
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Patent number: 4346223Abstract: This invention relates to the reduction of THP to perhydrophenanthridines (PHA) with formic acid. This is illustrated by the following equation ##STR1## where R is hydrogen or a substituted group, such as hydrocarbon, for example alkyl, etc.; and X and Y are hydrogen or a substituted group, such as a hydrocarbon group containing a functional group, for example alkyl-X where X is a functional group such as nitrilo, carboxyl, etc. The perhydrophenanthridines of this invention are useful as corrosion inhibitors and as fuel stability additives.Type: GrantFiled: May 18, 1981Date of Patent: August 24, 1982Assignee: Petrolite CorporationInventor: Bernardus A. Oude Alink
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Patent number: 4287337Abstract: The invention relates to spiropyran compounds. They have the general formula (I): ##STR1## in which: X represents the CH.sub.2 group or a sulfur atom; R.sub.1 and R.sub.2 represent electron donor and/or acceptor groups selected for instance from the group NO.sub.2, COC.sub.6 H.sub.5, CN, the halogens, the acyl substituents, alkoxy substituents, the hydrogen atom, the alkyl and mercaptoalkyl groups, the ethers of the formula CH.sub.2 OR, thioethers of the formula CH.sub.2 SR and amines of the formula CH.sub.2 NR.sub.2 in which R represents an alkyl group; R.sub.3 is a linear or branched alkyl group, having 1 to 18 carbon atoms, or an arylalkyl or alkenyl group.--R.sub.4,R.sub.5,R.sub.6,R.sub.7,R.sub.8 and R.sub.9 have one of the meanings indicated for R.sub.3 or represent, two by two, with the group in ortho position, a --(CH.sub.2).sub.n -- group in which n is a number between 5 and 10.R.sub.10 represents a hydrogen atom if X=S and if X=CH.sub.Type: GrantFiled: November 21, 1979Date of Patent: September 1, 1981Assignee: Etat Francais represente par le Delegue General pour l'ArmementInventors: Robert J. Guglielmetti, Francis Garnier, Yves M. Poirier, Gisele M. C. Petillon
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Patent number: 4273775Abstract: A series of novel tetrahydroquinoline-derived spiro-hydantoin compounds has been prepared, including their pharmaceutically acceptable acid addition salts. These particular compounds are useful in therapy as aldose reductase inhibitors for the control of certain chronic diabetic complications. Preferred member compounds include 1'-methyl-1',2',3',4'-tetrahydro-spiro-[imidazolidine-4,4'-quinoline]-2,5- dione, 6'-chloro-1',2',3',4'-tetrahydro-spiro-[imidazolidine-4,4'-quinoline]-2,5- dione, 7'-chloro-1',2',3',4'-tetrahydro-spiro-[imidazolidine-4,4'-quinoline]-2,5- dione and 1'-methyl-1',2',3',4'-tetrahydro-spiro-[imidazolidine-4,4'-pyrido(2,3-b)py ridine]-2,5-dione. Methods for preparing these compounds from known starting materials are provided.Type: GrantFiled: May 27, 1980Date of Patent: June 16, 1981Assignee: Pfizer Inc.Inventor: Reinhard Sarges
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Patent number: 4248882Abstract: A series of amino-and alkylamino-substituted spirohydantoins and pharmaceutically acceptable salts thereof useful as inhibitors of the enzyme aldose reductase and as therapeutic agents for the treatment of chronic complications associated with diabetes are disclosed. Preferred compounds include 6-chloro-8-amino-spiro[4H-2,3-dihydro-1-benzopyran-4,4'-imidazolidine]-2', 5'-dione, the 6-fluoro and 8-methylamino- analogs thereof and the corresponding dihydrobenzothiopyran analogs of these compounds. The optical isomers of these compounds having the 4S-configuration are especially preferred.Type: GrantFiled: February 12, 1980Date of Patent: February 3, 1981Assignee: Pfizer Inc.Inventors: Reinhard Sarges, Rodney C. Schnur
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Patent number: 4235911Abstract: A series of novel tetrahydroquinoline-derived spiro-hydantoin compounds has been prepared, including their pharmaceutically acceptable acid addition salts. These particular compounds are useful in therapy as aldose reductase inhibitors for the control of certain chronic diabetic complications. Preferred member compounds include 1'-methyl-1',2',3',4'-tetrahydro- spiro-[imidazolidine-4,4'-quinoline]-2,5-dione, 6'-chloro-1',2',3',4'-tetrahydro-spiro-[imidazolidine-4,4'-quinoline]-2,5- dione, 7'-chloro-1',2',3',4'-tetrahydro-spiro-[imidazolidine-4,4'-quinoline]-2,5- dione and 1'-methyl-1',2',3',4'-tetrahydro-spiro-[imidazolidine-4,4'-pyrido(2,3-b)py ridine]-2,5-dione. Methods for preparing these compounds from known starting materials are provided.Type: GrantFiled: June 13, 1979Date of Patent: November 25, 1980Assignee: Pfizer Inc.Inventor: Reinhard Sarges
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Patent number: 4222931Abstract: Stabilizers for organic polymeric materials are provided, comprising a phosphonic acid ester, a phenolic antioxidant and a 2,2,6,6-tetramethyl-4-piperidyl ether alcohol or ether having the general formula: ##STR1## wherein R.sub.2 is lower alkyl or hydroxyalkyl having from one to six carbon atoms;R.sub.3 is a hydrogen atom, provided R.sub.2 is hydroxyalkyl; ##STR2## R.sub.2 and R.sub.3 may be taken together to form ##STR3## Y is selected from the group consisting of hydrogen and O.Type: GrantFiled: December 8, 1977Date of Patent: September 16, 1980Assignee: Argus Chemical CorporationInventors: Motonobu Minagawa, Yutaka Nakahara, Naohiro Kubota, Toshihiro Shibata
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Patent number: 4200639Abstract: A novel alkaloid compound named "sesbanine" has been produced from the tissue of a leguminous plant known as Sesbania drummondii.Type: GrantFiled: March 29, 1979Date of Patent: April 29, 1980Assignee: The United States of America as represented by the Secretary of AgricultureInventor: Richard G. Powell
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Patent number: 4199589Abstract: N-(2-aminocycloheptyl)-N-alkanoylanilides and their 2-N-oxides of the formula ##STR1## e.g., trans-3,4-dichloro-N-[2-(dimethylamino)cycloheptyl]acrylanilide, and their pharmacologically acceptable salts, have been found to possess potent Central Nervous System anti-depressant properties. Many of them are new.These compounds are promising anti-depressant drugs which are characterized by lower toxicity than imipramine, and long acting activity which may allow longer durations between administrations, e.g., once a day. Pharmaceutical compositions containing these compounds and a process for treating conditions of depression with these compositions are disclosed.Type: GrantFiled: February 6, 1979Date of Patent: April 22, 1980Inventor: Jacob Szmuszkovicz
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Patent number: 4193996Abstract: Novel spiro-quinolone hydantoin derivatives useful as aldose reductase inhibitors and as therapeutic agents for the treatment of chronic diabetic complications are disclosed. Pharmaceutical compositions containing the novel compounds and a method of treating chronic diabetic complications are also disclosed. Preferred compounds include spiro[2,3-dihydro-1H,5H-benzo[ij]quinolizin[1,4']imidazolidin]-2',5,5.dbd. -trione and 10-chloro-spiro[2,3-dihydro-1H,5H-benzo[ij]quinolizin[1,4']imidazolidin]-2 ',5,5'-trione.Type: GrantFiled: April 4, 1979Date of Patent: March 18, 1980Assignee: Pfizer Inc.Inventor: Rodney C. Schnur
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Patent number: 4176185Abstract: Novel spiro-quinolylhydantoin derivatives useful as aldose reductase inhibitors and as therapeutic agents for the treatment of chronic diabetic complications are disclosed. Preferred compounds include spiro[imidazolidin-4,4'-pyrano[3,2-h]quinolin]-2,5-dione and spiro[imidazolidin-4,4'-pyrano[2,3-f]quinolin]-2,5-dione.Type: GrantFiled: January 22, 1979Date of Patent: November 27, 1979Assignee: Pfizer Inc.Inventor: Rodney C. Schnur
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Patent number: 4157398Abstract: N-(2-Aminocyclopentyl)N-alkanoylanilides and their 2-N-oxides of the formula ##STR1## e.g., trans-3,4-dichloro-N-[2-(dimethylamino)cyclopentyl]propionanilide, and their pharmacologically acceptable salts, have been found to possess potent Central Nervous System anti-depressant properties. Many of them are new.These compounds are promising anti-depressant drugs which are characterized by a better therapeutic ratio than imipramine, and long acting activity which may allow longer durations between administrations, e.g., once a day. Pharmaceutical compositions containing these compounds and a process for treating conditions of depression with these compositions are disclosed.Type: GrantFiled: February 21, 1978Date of Patent: June 5, 1979Assignee: The Upjohn CompanyInventor: Jacob Szmuszkovicz
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Patent number: 4128608Abstract: 2,2,6,6-TETRAMETHYL-4-PIPERIDYL SPIRO ALIPHATIC ETHERS ARE PROVIDED, USEFUL AS STABILIZERS FOR ORGANIC POLYMERIC MATERIALS, AND HAVING THE GENERAL FORMULA: ##STR1## wherein: R.sub.1 is selected from the group consisting of hydrogen, lower alkyl and lower hydroxyalkyl having one or two carbon atoms; ##STR2## R.sub.3 is selected from the group consisting of hydrogen and O; and n is 0 to 1.Type: GrantFiled: December 8, 1977Date of Patent: December 5, 1978Assignee: Argus Chemical CorporationInventors: Motonobu Minagawa, Naohiro Kubota, Toshihiro Shibata