Polycyclo Ring System Having The Six-membered Hetero Ring As One Of The Cyclos Patents (Class 546/18)
  • Patent number: 4771091
    Abstract: 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: Grant
    Filed: November 24, 1986
    Date of Patent: September 13, 1988
    Assignee: Hoechst Aktiengesellschaft
    Inventor: Josef Ertl
  • Patent number: 4731366
    Abstract: 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: Grant
    Filed: August 5, 1986
    Date of Patent: March 15, 1988
    Assignee: Harbor Branch Oceanographic Institution, Inc.
    Inventors: Murray H. G. Munro, Nigel B. Perry, John W. Blunt
  • Patent number: 4717724
    Abstract: 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: Grant
    Filed: March 8, 1984
    Date of Patent: January 5, 1988
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Wolfgang Schaper, Ernst Blume, Wolfgang Raether, Walter Dittmar
  • Patent number: 4710504
    Abstract: 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: Grant
    Filed: April 4, 1986
    Date of Patent: December 1, 1987
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, Joel R. Huff, Joseph P. Vacca, Steven D. Young, Jane deSolms, James P. Guare, Jr.
  • Patent number: 4652564
    Abstract: 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: Grant
    Filed: December 14, 1983
    Date of Patent: March 24, 1987
    Assignee: Schering Corporation
    Inventor: David J. Blythin
  • Patent number: 4623380
    Abstract: 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: Grant
    Filed: February 1, 1985
    Date of Patent: November 18, 1986
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Roland Schmierer, Reinhard Handte, Hilmar Mildenberger, Klaus Bauer, Hermann Bieringer, Helmut Burstell
  • Patent number: 4617305
    Abstract: 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: Grant
    Filed: February 22, 1984
    Date of Patent: October 14, 1986
    Assignee: Omnichem, S.A.
    Inventor: Jean A. A. J. Hannart
  • Patent number: 4617302
    Abstract: This invention provides certain pyridazinone derivatives, their pharmaceutical formulations, and their use as positive inotropic agents.
    Type: Grant
    Filed: October 15, 1984
    Date of Patent: October 14, 1986
    Assignee: Eli Lilly and Company
    Inventor: David W. Robertson
  • Patent number: 4600776
    Abstract: 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: Grant
    Filed: June 11, 1984
    Date of Patent: July 15, 1986
    Assignee: Bayer Aktiengesellschaft
    Inventors: Karlheinrich Meisel, Roderich Raue
  • Patent number: 4595754
    Abstract: 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: Grant
    Filed: March 4, 1985
    Date of Patent: June 17, 1986
    Assignee: Eli Lilly and Company
    Inventors: Randall K. Atkins, Leland O. Weigel
  • Patent number: 4575507
    Abstract: 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: Grant
    Filed: May 29, 1985
    Date of Patent: March 11, 1986
    Assignee: Pfizer Inc.
    Inventor: Christopher A. Lipinski
  • Patent number: 4556712
    Abstract: 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: Grant
    Filed: March 18, 1983
    Date of Patent: December 3, 1985
    Assignee: The United States of America as represented by the Secretary of the Department of Health and Human Services
    Inventor: Kenner C. Rice
  • Patent number: 4550112
    Abstract: 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: Grant
    Filed: September 16, 1983
    Date of Patent: October 29, 1985
    Assignee: Kali-Chemie Pharma GmbH
    Inventors: Uwe Schoen, Bernd Hachmeister, Wolfgang Kehrbach, Ulrich Kuehl, Gerd Buschmann
  • Patent number: 4537892
    Abstract: 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: Grant
    Filed: September 14, 1983
    Date of Patent: August 27, 1985
    Assignee: Alcon Laboratories, Inc.
    Inventor: Billie M. York, Jr.
  • Patent number: 4503066
    Abstract: 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: Grant
    Filed: May 11, 1982
    Date of Patent: March 5, 1985
    Assignee: Imperial Chemical Industries PLC
    Inventors: David R. Brittain, Robin Wood
  • Patent number: 4410700
    Abstract: 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: Grant
    Filed: May 20, 1981
    Date of Patent: October 18, 1983
    Assignee: The United States of America as represented by the Department of Health and Human Services
    Inventor: Kenner C. Rice
  • Patent number: 4410699
    Abstract: 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: Grant
    Filed: November 29, 1982
    Date of Patent: October 18, 1983
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Richard C. Effland, Larry Davis, Joseph T. Klein
  • Patent number: 4374137
    Abstract: 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: Grant
    Filed: August 7, 1981
    Date of Patent: February 15, 1983
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Richard C. Effland, Larry Davis, Joseph T. Klein
  • Patent number: 4346223
    Abstract: 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: Grant
    Filed: May 18, 1981
    Date of Patent: August 24, 1982
    Assignee: Petrolite Corporation
    Inventor: Bernardus A. Oude Alink
  • Patent number: 4287337
    Abstract: 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: Grant
    Filed: November 21, 1979
    Date of Patent: September 1, 1981
    Assignee: Etat Francais represente par le Delegue General pour l'Armement
    Inventors: Robert J. Guglielmetti, Francis Garnier, Yves M. Poirier, Gisele M. C. Petillon
  • Patent number: 4273775
    Abstract: 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: Grant
    Filed: May 27, 1980
    Date of Patent: June 16, 1981
    Assignee: Pfizer Inc.
    Inventor: Reinhard Sarges
  • Patent number: 4248882
    Abstract: 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: Grant
    Filed: February 12, 1980
    Date of Patent: February 3, 1981
    Assignee: Pfizer Inc.
    Inventors: Reinhard Sarges, Rodney C. Schnur
  • Patent number: 4235911
    Abstract: 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: Grant
    Filed: June 13, 1979
    Date of Patent: November 25, 1980
    Assignee: Pfizer Inc.
    Inventor: Reinhard Sarges
  • Patent number: 4222931
    Abstract: 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: Grant
    Filed: December 8, 1977
    Date of Patent: September 16, 1980
    Assignee: Argus Chemical Corporation
    Inventors: Motonobu Minagawa, Yutaka Nakahara, Naohiro Kubota, Toshihiro Shibata
  • Patent number: 4200639
    Abstract: A novel alkaloid compound named "sesbanine" has been produced from the tissue of a leguminous plant known as Sesbania drummondii.
    Type: Grant
    Filed: March 29, 1979
    Date of Patent: April 29, 1980
    Assignee: The United States of America as represented by the Secretary of Agriculture
    Inventor: Richard G. Powell
  • Patent number: 4199589
    Abstract: 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: Grant
    Filed: February 6, 1979
    Date of Patent: April 22, 1980
    Inventor: Jacob Szmuszkovicz
  • Patent number: 4193996
    Abstract: 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: Grant
    Filed: April 4, 1979
    Date of Patent: March 18, 1980
    Assignee: Pfizer Inc.
    Inventor: Rodney C. Schnur
  • Patent number: 4176185
    Abstract: 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: Grant
    Filed: January 22, 1979
    Date of Patent: November 27, 1979
    Assignee: Pfizer Inc.
    Inventor: Rodney C. Schnur
  • Patent number: 4157398
    Abstract: 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: Grant
    Filed: February 21, 1978
    Date of Patent: June 5, 1979
    Assignee: The Upjohn Company
    Inventor: Jacob Szmuszkovicz
  • Patent number: 4128608
    Abstract: 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: Grant
    Filed: December 8, 1977
    Date of Patent: December 5, 1978
    Assignee: Argus Chemical Corporation
    Inventors: Motonobu Minagawa, Naohiro Kubota, Toshihiro Shibata