Single Bond Between 1,2-positions And Single Bond Between 3,4-positions Patents (Class 546/165)
-
Patent number: 4771059Abstract: The subject compounds, which are adapted for the site-specific/sustained delivery of centrally acting drug species to the brain, are compounds of the formula ##STR1## and the non-toxic pharmaceutically acceptable salts thereof, wherein D is the residue of a centrally acting primary, secondary or tertiary amine and ##STR2## is an unsubstituted or substituted dihydropyridyl, dihydroquinolyl or dihydroisoquinolyl radical. The corresponding ionic pyridinium, quinolinium and isoquinolinium salts ##STR3## X.sup.-, wherein X.sup.- is the anion of a non-toxic pharmaceutically acceptable acid, are also disclosed.Type: GrantFiled: August 29, 1985Date of Patent: September 13, 1988Assignee: University of FloridaInventor: Nicholas S. Bodor
-
Patent number: 4760057Abstract: This invention relates to novel (acyloxyalkoxy)carbonyl derivatives as bioreversible prodrug moieties for primary and secondary amine functions in drugs having a primary or secondary amine function thereon. Hydrolytic enzymes are used to trigger the regeneration of the parent amine drug of the carbamate prodrug moiety. The case also contains pharmaceutical composition, method of treatment and process claims.Type: GrantFiled: April 22, 1985Date of Patent: July 26, 1988Assignee: Merck & Co., Inc.Inventor: Jose Alexander
-
Patent number: 4749698Abstract: Compounds having the general structure ##STR1## and their pharmaceutically acceptable salts, wherein the substituents are defined herein, which exhibit antihypertensive activity.Type: GrantFiled: July 8, 1985Date of Patent: June 7, 1988Assignee: Rorer Pharmaceutical CorporationInventors: Edward S. Neiss, John T. Suh, John R. Regan, Jerry W. Skiles, Jeffrey N. Barton, James J. Mencel, Paul Menard
-
Patent number: 4740600Abstract: Surfactants which are blocked against surfactant action (identified herein as "photolabile blocked surfactants") by a photolabile protective or masking group but which, on exposure to actinic radiation, become unblocked are provided. Coating compositions in which surfactant is formed on irradiation are provided by blending the photolabile blocked surfactant with polymeric film-forming materials.Compositions containing the photolabile blocked surfactants are useful when employed as protective coatings on various substrates or as the adhesive in a pressure sensitive adhesive tape. Although initially well adhering to a substrate, such compositions may be readily removed from the substrate following exposure of the same to suitable radiation which unblocks the surfactant to permit it to regain its surfactant activity.Type: GrantFiled: January 6, 1986Date of Patent: April 26, 1988Assignee: Minnesota Mining and Manufacturing CompanyInventors: Gilbert L. Eian, John E. Trend
-
Patent number: 4738972Abstract: Hypoglycemic 5-[1-(5,6,7,8-tetrahydro-2-napthyl-; 1,2,3,4-tetrahydro-6-quinolyl-; 2-indanyl-; and 2-indolyl)alkyl]thiazolidine-2,4-dione derivatives, pharmaceutically acceptable salts thereof, and a method for their use in the treatment of hyperglycemic mammals.Type: GrantFiled: June 26, 1987Date of Patent: April 19, 1988Assignee: Pfizer Inc.Inventors: James F. Eggler, Gerald F. Holland, Michael R. Johnson, Robert A. Volkmann
-
Patent number: 4731105Abstract: Herbicidal thiadiazolyloxyacetamides of the formula: ##STR1## wherein: R is an optionally-substituted alkyl, cycloalkyl or aryl group; R.sup.1 and R.sup.2, which may be the same or different, each represent hydrogen, alkyl, cycloalkyl, alkoxy, alkenyl, aryl, aralkyl or aryloxy, any alkyl or aryl moiety thereof being optionally substituted; or R.sup.1 and R.sup.2, together with the nitrogen atom to which they are attached, represent a heterocyclic or benzheterocyclic group, the hetrocyclic ring of which is 5- or 6-membered, and which may be substituted by one or more alkyl groups; and X is oxygen, sulphur or --S(O).sub.n --where n is 1 or 2,process for their preparation, and compositions containing them.Type: GrantFiled: August 13, 1986Date of Patent: March 15, 1988Assignee: FBC LimitedInventor: Graham P. Jones
-
Patent number: 4727079Abstract: A brain-specific dopaminergic response is elicited in a patient in need of such treatment, e.g., a patient afflicted with Parkinson's disease of hyperprolactinemia, by administering thereto a therapeutically effective amount of preferably catechol protected dopamine tethered to a reduced, blood-brain barrier penetrating lipoidal form [D-DHC] of a dihydropyridine.revreaction.pyridinium salt type redox carrier, e.g., 1,4-dihydrotrigonelline. Oxidation of the dihydropyridine carrier moiety in vivo to the ionic pyridinium salt type dopamine/carrier entity [D-QC].sup.+ prevents elimination thereof from the brain, while elimination from the general circulation is accelerated, resulting in significant and prolongedly sustained brain-specific dopaminergic activity.Type: GrantFiled: May 13, 1985Date of Patent: February 23, 1988Assignee: University of FloridaInventor: Nicholas S. Bodor
-
Patent number: 4723007Abstract: The invention relates to benzopyrrolobenzodiazepines and quinobenzodiazepines of the formula ##STR1## where X and Y may be the same or different and each is hydrogen, halogen, CF.sub.3, lower alkyl, lower alkoxy, lower alkylthio and lower alkylsulfonyl, p and q are independently 1 or 2; R.sub.1 is hydrogen when R.sub.2 is bonded to R.sub.3 to form a --(CH.sub.2).sub.m --CH.sub.2 -- group or a --CH.dbd.CH-- group; R.sub.3 is hydrogen when R.sub.1 is bonded to R.sub.2 to form a --(CH.sub.2).sub.m --CH.sub.2 -- group or a --CH.dbd.CH-- group; m is 1 or 2; R.sub.4 is NR.sub.5 R.sub.6 wherein R.sub.5 is hydrogen or lower alkyl and R.sub.6 is hydrogen, lower alkyl or a group of the formula (CH.sub.2).sub.n NR.sub.7 R.sub.8 wherein R.sub.7 and R.sub.8 are lower alkyl, and n is 2 or 3, ##STR2## wherein R.sub.9 is lower alkyl, ##STR3## wherein R.sub.10 is CH.sub.2 CH.sub.2 OH, lower alkyl, phenyl, phenyl substituted by halogen, CF.sub.Type: GrantFiled: November 12, 1986Date of Patent: February 2, 1988Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Edward J. Glamkowski, Yulin Chiang
-
Patent number: 4723014Abstract: The present invention provides a process for preparing a 2-substituted-1,4-dihydropyridine by providing a regiospecific bromine containing intermediate which is then reacted with a nucleophile to provide a wide range of substituents at the 2-position of 1,4-dihydropyridines. Also the present invention is novel 3-substituted-1,4-dihydropyridines having cardiovascular activity.Type: GrantFiled: November 19, 1986Date of Patent: February 2, 1988Assignee: Warner-Lambert CompanyInventors: Kevin R. Anderson, Ila Sircar
-
Patent number: 4703044Abstract: The invention provides novel imidazoquinolines, processes for their preparation and pharmaceutical compositions containing them. The compounds have Formula I ##STR1## wherein A is a C.sub.1 -C.sub.4 straight or branched alkylene chain which may be saturated or unsaturated,B is a C.sub.2 -C.sub.4 straight or branched alkylene chain which may be saturated or unsaturated,R.sup.1 and R.sup.2 are the same or different and are hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkoxyalkyl, C.sub.1-6 hydroxyalkyl, hydroxy, halogen, nitro, carboxy, carboxylic lower alkyl ester, carbamoyl, carbamoyloxy, cyano, loweralkanoyl, lower alkanoylamino or trifluoromethyl, Het is a heterocyclic group chosen from imidazolyl, imidazolinyl, benzimidazolyl, thiazolyl, thiazolinyl, quinolyl, piperidyl, pryidyl, benzothiazoly and pyrimidyl, any of which heterocyclic groups may be substituted, and x is 0 or 1, and pharmaceutically acceptable salts thereof.The compounds are anti-ulcer/anti-secretory agents.Type: GrantFiled: December 11, 1985Date of Patent: October 27, 1987Assignee: John Wyeth & Brother LimitedInventor: Roger Crossley
-
Patent number: 4691016Abstract: The compounds 8-bromo-6,7-dihydro-9-fluoro-5-methyl-1-oxo-1H,5H-benzo[ij]quinolizine-2-c arboxylic acid and 8-chloro-6,7-dihydro-9-fluoro-5-methyl-1-oxo-1H,5H-benzo[ij]quinolizine-2- carboxylic acid are disclosed as potent antimicrobials. Pharmaceutically-acceptable carboxylate salts, acyl chlorides, esters and alkylaminoalkyl ester salts of the acids are also disclosed.Type: GrantFiled: August 22, 1985Date of Patent: September 1, 1987Assignee: Riker Laboratories, Inc.Inventor: Richard M. Stern
-
Patent number: 4665023Abstract: The present invention provides imidazole derivatives of the general formula: ##STR1## wherein R, R.sub.1 and R.sub.2 are defined hereinbelow. The present invention is also concerned with processes for the preparation of these imidazole derivatives and with the use thereof as redox indicators.Type: GrantFiled: March 29, 1985Date of Patent: May 12, 1987Assignee: Boehringer Mannheim GmbHInventors: Ulfert Deneke, Werner Guthlein, Manfred Kuhr, Hartmut Merdes, Hans-Rudiger Murawski, Hans Wielinger
-
Patent number: 4658025Type: GrantFiled: December 21, 1984Date of Patent: April 14, 1987Assignee: Bayer AktiengesellschaftInventor: Fritz Maurer
-
Patent number: 4647667Abstract: A 1-substituted-3-permissibly-substituted-6 (or 7)-oxodecahydroquinoline is converted to the corresponding 7 (or 6)-formyl derivative. The 6-oxo-7-formyl compound, upon treatment with hydrazine, is cyclized to a tautomeric mixture of 5-substituted-7-permissibly-substituted-4,4a,5,6,7,8,8a,9-octahydro-1H(and 2H)-pyrazolo[3,4-g]quinolines.Type: GrantFiled: September 16, 1985Date of Patent: March 3, 1987Assignee: Eli Lilly and CompanyInventor: John M. Schaus
-
Patent number: 4645525Abstract: Azolyloxy-carboxylic acid amides of the formula ##STR1## wherein R is a five-membered hetero-aromatic monocyclic radical which contains an oxygen atom or a sulfur atom and 1 to 3 nitrogen atoms; orR is said monocyclic radical substituted by halogen, nitro, cyano, amino, alkylamino, dialkylamino, arylamino, alkylcarbonylamino, alkylcarbonyl, carboxyl, alkoxycarbonyl, carbamoyl, alkylaminocarbonyl, dialkylaminocarbonyl, arylaminocarbonyl substituted arylaminocarbonyl wherein the substituents are halogen, nitro or alkyl, aryl, substituted aryl wherein the substituents are halogen, nitro, cyano, alkyl, halogenoalkyl or alkoxy, aralkyl, haloaralkyl, alkoxy, halo-alkoxy, alkenoxy, alkynoxy, alkoxycarbonylalkoxy, aralkoxy or aryloxy, optionally halogen-substituted alkylthio, alkenylthio, alkynylthio, alkoxycarbonylalkylthio, aralkylthio, arylthio, alkylsulphinyl or alkylsulphonyl, optionally halogen-substituted alkyl, alkenyl, alkynyl, alkoxyalkyl, aralkoxyalkyl, aryloxyalkyl, alkylthioalkyl, alkylsulphinylalkyl, alType: GrantFiled: August 26, 1983Date of Patent: February 24, 1987Assignee: Bayer AktiengesellschaftInventors: Heinz Forster, Wolfgang Hofer, Volker Mues, Ludwig Eue, Robert R. Schmidt
-
Patent number: 4634715Abstract: There are disclosed aza analogs of carboxyalkyl dipeptide derivatives and related compounds which are useful as converting enzyme inhibitors and as antihypertensives said compounds being represented by the general formula: ##STR1## wherein A and B can be joined together to form various ring structures.Type: GrantFiled: July 27, 1983Date of Patent: January 6, 1987Assignee: Merck & Co., Inc.Inventors: William J. Greenlee, Eugene D. Thorsett
-
Patent number: 4634713Abstract: Certain 3-(ureidocyclohexyleneamino)propane-1,2-diol derivatives, such as the compounds of formula III below, represent novel and useful pharmaceutical agents, e.g. potent antihypertensive and cardioactive agents demonstrating both .alpha.- and .beta.-adrenergic blocking activity. ##STR1## R.sub.3 is hydrogen or lower alkyl; R.sub.7 is cyano, lower alkoxycarbonyl, pyrrolyl, morpholino, alkenyloxy of 3 to 6 carbon atoms, alkynyloxy of 3 to 6 carbon atoms, alkoxy of 1 to 3 carbon atoms substituted by cyclopropyl.Type: GrantFiled: August 19, 1985Date of Patent: January 6, 1987Assignee: Ciba-Geigy CorporationInventors: Lincoln H. Werner, Neville Ford
-
Patent number: 4626591Abstract: A process for preparing 1-alkyl-6-oxodecahydroquinolines in 5 steps--a quaternization, hydrogenation, two organometallic reductions and hydrolysis of the thus formed enol ether--from 6-alkyloxyquinoline and intermediates useful therein.Type: GrantFiled: April 19, 1985Date of Patent: December 2, 1986Assignee: Eli Lilly and CompanyInventor: John M. Schaus
-
Patent number: 4623377Abstract: Tetrahydroquinolin-1-ylcarbonylimidazoles of the formula ##STR1## in which n is 0, 1, 2 or 3,which possess herbicidal and fungicidal activity. The corresponding intermediates of the formula ##STR2## are also new.Type: GrantFiled: April 19, 1985Date of Patent: November 18, 1986Assignee: Nihon Tokushu Noyaku Seizo K.K.Inventors: Yoshio Kurahashi, Kozo Shiokawa, Toshio Goto, Shinzo Kagabu, Atsumi Kamochi, Koichi Moriya, Hidenori Hayakawa
-
Patent number: 4622399Abstract: Herein is disclosed bicyclic-substituted aminoethanol derivatives, therapeutically acceptable acid addition salts thereof, processes for their preparation, methods of using the derivatives and pharmaceutical compositions. The derivatives are useful for treating hypertension in a mammal.Type: GrantFiled: May 23, 1985Date of Patent: November 11, 1986Assignee: American Home Products CorporationInventors: Andre A. Asselin, Danilo A. Crosilla, Leslie G. Humber
-
Patent number: 4619784Abstract: There are disclosed diffusion transfer color processes and products which employ novel image dye-providing materials which provide image dyes having the chromophoric system represented by the formula ##STR1## X is H, alkyl, aryl or substituted aryl; W is H or alkyl, R is H or alkyl; m and n are each integers of from 2 to 6.The image dye-providing material includes a diffusion control moiety such as a hydroquinonyl group and may be diffusible or nondiffusible as a function of the diffusion control moiety.Type: GrantFiled: October 27, 1980Date of Patent: October 28, 1986Assignee: Polaroid Corporation, Patent Dept.Inventors: Louis Locatell, Jr., Charles M. Zepp, Ronald F. Cieciuch
-
Patent number: 4617395Abstract: Quinoline and substituted quinolines are prepared by reacting aniline or a substituted aniline with an .alpha., .beta.-monounsaturated aldehyde in a high-boiling mineral oil by a method in which the high-boiling mineral oil is replaced when it becomes enriched with by-products, and the said mineral oil enriched with by-products is removed.Type: GrantFiled: October 15, 1984Date of Patent: October 14, 1986Assignee: BASF AktiengesellschaftInventors: Toni Dockner, Helmut Hagen, Herbert Krug
-
Patent number: 4603199Abstract: Antimicrobial compounds of the following formula are disclosed: ##STR1## wherein X is selected from the group consisting of --O--, --CH.sub.2 and ##STR2## m is 0 or 1; R.sub.1 is selected from the group consisting of hydrogen, nitro, amino, lower alkyl, lower alkanamido, lower N,N-dialkylamino, formamido, hydroxy, lower alkoxy, halogen, lower haloalkanamido and pyrryl; n is 1 or 2; and R.sub.2 is selected from the group consisting of hydrogen, methyl, fluoro, chloro and nitro. Acyl chlorides, esters, alkylaminoalkyl ester salts, amides and pharmaceutically acceptable carboxylate salts are also disclosed. Pharmaceutical compositions containing these compounds, methods of using these compound and synthetic intermediates are also disclosed.Type: GrantFiled: January 26, 1984Date of Patent: July 29, 1986Assignee: Riker Laboratories, Inc.Inventors: John F. Gerster, Richard M. Stern
-
Patent number: 4602002Abstract: Compounds of the formula: ##STR1## wherein R.sup.2 is --(CH.sub.2).sub.k --X--(CH.sub.2).sub.j --NHR.sup.3 ; wherein k is 0 to 3, j is 1 or 2; X is F or OH; and, R.sup.3 is hydrogen; loweralkyl or loweraralkyl which may be substituted by hydroxy, carboxy, carbamoyl, or carbalkoxy; or, acyl; and, a pharmaceutically acceptable salt thereof; are inhibitors of angiotensin I converting enzyme useful as antihypertensive agents.Type: GrantFiled: February 7, 1983Date of Patent: July 22, 1986Assignee: Merck & Co., Inc.Inventors: Arthur A. Patchett, Mu T. Wu
-
Patent number: 4599410Abstract: Methine dyes are disclosed which contain a 2-halo or pseudohalo substituted 1,2,5-oxatellurazole ring fused with an aromatic nucleus, the aromatic nucleus being substituted with a methine linkage terminating in an auxochrome providing a conjugated resonance chromophore. The dyes can be formed by condensing a methine linkage precursor with a compound containing an oxatellurazole ring fused with an aromatic nucleus. The dyes are useful in optical recording elements and in photographic elements.Type: GrantFiled: February 19, 1985Date of Patent: July 8, 1986Assignee: Eastman Kodak CompanyInventor: Wolfgang H. H. Gunther
-
Patent number: 4598151Abstract: Dyestuffs of the formula ##STR1## wherein R represents hydrogen or optionally substituted alkyl,A represents ##STR2## wherein R.sup.1 represents hydrogen, optionally substituted alkyl or cycloalkyl andR.sup.2 represents optionally substituted alkyl which can close a ring to ring B, aralkyl or aryl orR.sup.1 and R.sup.2, together with the N atom, form a ring,D and E represent hydrogen, optionally substituted alkyl or alkenyl and D additionally represents aryl, aralkyl, aralkenyl or a heterocyclic radical, or D and E, together with the C atom, form a ring andAn.sup.- represents an anion,are used for pulp-coloring paper and dyeing cationically dyeable fibres.Type: GrantFiled: November 15, 1982Date of Patent: July 1, 1986Assignee: Bayer AktiengesellschaftInventors: Hans-Peter Kuhlthau, Horst Harnisch
-
Patent number: 4596871Abstract: Tautomeric mixtures of trans-(.+-.)-3,5-dialkyloctahydropyrazolo[3,4-g]quinoline, of trans-(.+-.)-6-alkyloctahydropyrazolo[4,3-f]quinoline, and of trans-(.+-.)-1,6-dialkyloctahydropyrazolo[4,3-f]quinoline, individual enantiomer thereof, pharmaceutically-acceptable acid addition salts thereof, and intermediates useful in the preparation thereof, useful as hypotensive agents.Type: GrantFiled: April 3, 1985Date of Patent: June 24, 1986Assignee: Eli Lilly and CompanyInventors: John M. Schaus, Diane L. Huser, Richard N. Booher
-
Patent number: 4587296Abstract: Additives for rubber compositions, giving vulcanisates having improved retention of optimum physical properties, are compounds containing two or more groups of the formula --S--SO.sub.2 R linked by an organic bridging group, or polymers containing two or more groups of the formula --S--SO.sub.2 R attached to an organic polymer chain, where R represents (a) a radical OM where M is a monovalent metal, the equivalent of a multivalent metal, a monovalent in derived by the addition of a proton to a nitrogenous base, or the equivalent of a multivalent ion derived by the addition of two or more protons to a nitrogenous base, or (b) an organic radical selected from aliphatic, cycloaliphatic, aromatic and heterocyclic radicals, and radicals which are combinations of any two or more such radicals.Type: GrantFiled: April 11, 1985Date of Patent: May 6, 1986Assignee: Monsanto Europe, S.A.Inventor: Philippe G. Moniotte
-
Patent number: 4585471Abstract: Substituted 5-trifluoromethyl-1,3,4-thiadiazol-2-yl-oxyacetic acid amides of the formula ##STR1## in which R.sup.1 and R.sup.2 are identical or different and each represent alkyl, alkenyl, alkinyl, alkoxy, aralkyl, cycloalkyl, cycloalkenyl or aryl, each of which is optionally substituted, or a nitrogen-containing heterocyclic radical, or, together with the nitrogen atom to which they are bonded, form an optionally substituted, optionally partially unsaturated and optionally benzo-fused monocyclic or bicyclic structure which optionally contains further hetero atoms, with the proviso that R.sub.1 does not represent methyl when R.sup.2 represents phenyl, which possess herbicidal activity.Type: GrantFiled: May 10, 1985Date of Patent: April 29, 1986Assignee: Bayer AktiengesellschaftInventors: Heinz Forster, Wolfgang J. Hofer, deceased, Robert R. Schmidt, Ludwig Eue
-
Patent number: 4585868Abstract: The compounds 5-carboxyl-6-fluoroquinaldine, 6-fluoro-5-methylquinaldine, 6-fluoro-5-methyl-1,2,3,4-tetrahydroquinaldine, 1,2-dihydro-6-fluoro-5-hydroxymethylquinaldine and diethyl 2-[N-(6-fluoro-5-methyl-1,2,3,4-tetrahydroquinaldinyl)]methylenemalonate are disclosed as useful intermediates for preparing the antimicrobial agent 6,7-dihydro-5,8-dimethyl-9-fluoro-1-oxo-1H,5H-benzol[ij]quinolizine- 2-carboxylic acid.Type: GrantFiled: June 25, 1984Date of Patent: April 29, 1986Assignee: Riker Laboratories, Inc.Inventor: Richard M. Stern
-
Patent number: 4584285Abstract: (Benzothiadiazine, benzamido and benzenesulfonyl)phenyl-substituted carboxyalkyl dipeptide compounds are disclosed. Compounds of this invention are useful as antihypertensive agents.Type: GrantFiled: September 17, 1984Date of Patent: April 22, 1986Assignee: Schering CorporationInventors: Ronald J. Doll, Bernard R. Neustadt, Elizabeth M. Smith, Charles V. Magatti, Elijah H. Gold
-
Patent number: 4577024Abstract: Oxoindolizine and oxoindolizinium dyes are novel compounds useful in imaging, such as laser recording and reading. These dyes are formed by (1) the reaction of a cyclopropenone and a pyridine compound, (2) by reaction of (a) color-forming couplers with (b) reaction products from the reaction of cyclopropenones with pyridine compounds, or (3) by condensation reactions of indolizinols, indolizinones, and indolizinium ions.Type: GrantFiled: August 27, 1982Date of Patent: March 18, 1986Assignee: Eastman Kodak CompanyInventors: George L. Fletcher, Jr., Steven L. Bender, Donald H. Wadsworth
-
Patent number: 4568750Abstract: The compounds 5-bromo-6-fluoroquinaldine, 5-bromo-6-fluoro-1,2,3,4-tetrahydroquinaldine, 1-acetyl-5-bromo-6-fluoro-1,2,3,4-tetrahydroquinaldine and diethyl 2-[N-(6-fluoro-5-methoxy-1,2,3,4-tetrahydroquinaldinyl)]-methylenemalonate are intermediates for preparing antimicrobial 8-alkoxy-6,7-dihydro-5-methyl-9-fluoro-1-oxo-1H,5H-benzo[ij]-quinolizine-2 -carboxylic acids.Type: GrantFiled: June 25, 1984Date of Patent: February 4, 1986Assignee: Riker Laboratories, Inc.Inventor: Richard M. Stern
-
Patent number: 4565871Abstract: Trans-(.+-.) or trans-(-)-2,4-permissibly-substituted-6-alkyl or allyl octahydropyrimido[4,5-g]quinolines and related compounds, ultraviolet light absorbers.Type: GrantFiled: December 11, 1984Date of Patent: January 21, 1986Assignee: Eli Lilly and CompanyInventors: Cynthia L. Nicholas, Edmund C. Kornfeld, John M. Schaus
-
Patent number: 4565872Abstract: A process for preparing 8-cyano-6,7-dihydro-5-methyl-1-oxo-1H,5H-benzo[ij]quinolizine-2-carboxylic acids from substituted benzoic acids. Intermediates involved in the process are also described. 8-cyano-6,7-dihydro-5-methyl-1-oxo-1H,5H-benzo[ij]quinolizine-2-carboxylic acids are antimicrobial agents.Type: GrantFiled: October 26, 1983Date of Patent: January 21, 1986Assignee: Riker Laboratories, Inc.Inventor: Charles M. Leir
-
Patent number: 4562200Abstract: Herein is disclosed bicyclic-substituted aminoethanol derivatives, therapeutically acceptable acid addition salts thereof, processes for their preparation, methods of using the derivatives and pharmaceutical compositions. The derivatives are useful for treating hypertension in a mammal.Type: GrantFiled: October 23, 1984Date of Patent: December 31, 1985Assignee: American Home Products CorporationInventors: Andre A. Asselin, Danilo A. Crosilla, Leslie G. Humber
-
Patent number: 4556713Abstract: The compounds 8-bromo-6,7-dihydro-9-fluoro-5-methyl-1-oxo-1H,5H-benzo[ij]quiniolizine-2- carboxylic acid and 8-chloro-6,7-dihydro-9-fluoro-5-methyl-1-oxo-1H,5H,-benzo[ij]quinolizine-2 -carboxylic acid are disclosed as potent antimicrobials. Pharmaceutically-acceptable carboxylate salts, acyl chlorides, esters and alkylaminoalkyl ester salts of the acids are also disclosed.Type: GrantFiled: November 15, 1984Date of Patent: December 3, 1985Assignee: Riker Laboratories, Inc.Inventor: Richard M. Stern
-
Patent number: 4549899Abstract: A substituted 3-trihalogenomethyl-1,2,4-thiadiazol-5-yl-oxyacetamide of the formula ##STR1## in which x represents --CFCl.sub.2, --CF.sub.2 Cl or --CF.sub.3 and R.sup.1 and R.sup.2 are identical or different and individually represent optionally substituted alkyl, alkenyl, alkinyl, alkoxy, aralkyl, cycloalkyl, cycloalkenyl, aryl or a nitrogen-containing heterocyclic radical, or, together with the nitrogen atom to which they are bonded, form an optionally substituted, optionally partially unsaturated and optionally benzofused monocyclic or bicyclic structure which optionally contains further hetero atoms, which possesses herbicidal activity.Type: GrantFiled: July 20, 1983Date of Patent: October 29, 1985Assignee: Bayer AktiengesellschaftInventors: Heinz Forster, Erich Klauke, Ludwig Eue, Robert R. Schmidt, Klaus Lurssen
-
Patent number: 4546099Abstract: The invention relates to novel N-aminomethyl-3-phenyl-4-cyanopyrrole derivatives of the formula I ##STR1## wherein R.sub.1 and R.sub.2 are each independently hydrogen, halogen, methoxy or methylthio,Z is a group ##STR2## wherein R.sub.3 and R.sub.4 are each independently hydrogen, C.sub.1 -C.sub.6 alkyl which is unsubstituted or substituted by cyano, C.sub.1 -C.sub.6 alkoxy or C.sub.1 -C.sub.6 alkoxycarbonyl; or are C.sub.3 -C.sub.6 alkenyl, C.sub.3 -C.sub.6 alkynyl, C.sub.3 -C.sub.7 cycloalkyl, benzyl or benzyl which is substituted by halogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 haloalkyl and/or C.sub.1 -C.sub.6 alkoxy, or phenyl or phenyl which is substituted by halogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 haloalkyl and/or C.sub.1 -C.sub.6 alkoxy, with the proviso that only one of R.sub.3 or R.sub.4 can be hydrogen,R.sub.5 and R.sub.6 are each independently hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.Type: GrantFiled: July 18, 1984Date of Patent: October 8, 1985Assignee: Ciba-Geigy CorporationInventor: Robert Nyfeler
-
Patent number: 4540430Abstract: A substituted 3-trichloromethyl-1,2,4-thiadiazol-5-yl-oxyacetamide of the formula ##STR1## in which R.sup.1 and R.sup.2 are identical or different and individually represent optionally substituted alkyl, alkenyl, alkinyl, alkoxy, aralkyl, cycloalkyl, cycloalkenyl, aryl or a nitrogen-containing heterocyclic radical, or, together with the nitrogen atom to which they are bonded, form an optionally substituted, optionally partially unsaturated and optionally benzo-fused monocyclic or bicyclic structure which optionally contains further heteroatoms,which possesses herbicidal activity.Type: GrantFiled: July 18, 1983Date of Patent: September 10, 1985Assignee: Bayer AktiengesellschaftInventors: Heinz Forster, Hans-Joachim Diehr, Jorg Stetter, Ludwig Eue, Robert R. Schmidt
-
Patent number: 4540780Abstract: Novel chemical compounds which are diphenylmethylene piperidine compounds are provided, as well as methods for their production, pharmaceutical compositions comprising the compounds, and methods of treatment using the compounds in dosage form. The compounds have both anticholinergic and antidopaminergic properties, and are useful as antiemetic, antihistamine, pulmonary, antiallergy, and antispasmodic agents.Type: GrantFiled: June 2, 1983Date of Patent: September 10, 1985Assignee: Warner-Lambert CompanyInventors: David A. Downs, Haile Tecle
-
Patent number: 4528379Abstract: In a process for the preparation of a substituted thiadiazolyloxyacetamide of the formula ##STR1## in which R.sup.1 and R.sup.2 each independently is hydrogen, alkyl, alkenyl, alkenyl, alkinyl, optionally substituted cycloalkyl or cycloalkenyl, halogenoalkyl, alkoxyalkyl, alkoxy, aralkyl or optionally substituted aryl, orR.sup.1 and R.sup.2, together with the nitrogen atom to which they are bonded, form an optionally substituted heterocyclic structure which can contain further hetero atoms,One of X and Y is a nitrogen atom and the other a C-R.sup.3 a grouping, andR.sup.Type: GrantFiled: July 18, 1983Date of Patent: July 9, 1985Assignee: Bayer AktiengesellschaftInventors: Reimer Colln, Karl H. Mohrmann
-
Patent number: 4524148Abstract: The compounds 8-bromo-6,7-dihydro-9-fluoro-5-methyl-1-oxo-1H,5H-benzo[ij]quiniolizine-2- carboxylic acid and 8-chloro-6,7-dihydro-9-fluoro-5-methyl-1-oxo-1H,5H,-benzo[ij]quinolizine-2 -carboxylic acid are disclosed as potent antimicrobials. Pharmaceutically-acceptable carboxylate salts, acyl chlorides, esters and alkylaminoalkyl ester salts of the acids are also disclosed.Type: GrantFiled: November 6, 1981Date of Patent: June 18, 1985Assignee: Riker Laboratories, Inc.Inventor: Richard M. Stern
-
Patent number: 4507478Abstract: Trans-(.+-.) or trans-(-)-2,4-permissibly-substituted-6-alkyl or allyl octahydropyrimido[4,5-g]quinolines and related compounds, ultraviolet light absorbers.Type: GrantFiled: September 26, 1983Date of Patent: March 26, 1985Assignee: Eli Lilly and CompanyInventors: Cynthia L. Nichols, Edmund C. Kornfeld, John M. Schaus
-
Patent number: 4506079Abstract: Convenient intermediates for preparing 3-substituted-2-hydroxypropyl aryl ether .beta.-blockers, a reaction to the intermediates of the following formula and a conversion to obtain the said .beta.-blockers are disclosed. ##STR1## (wherein X is hydrogen or halogen;Y is halogen, hydroxy, lower acyloxy, amino, lower alkylamino, lower aralkylamino, lower acylamino, di-lower alkylamino, lower alkyleneamino, N-lower alkyl-N-lower aralkylamino, di-lower acylamino, N-lower alkyl-N-lower acylamino or N-tri-lower alkylsilylamino;one of P and R combined together with Q represents lower alkylene or alkenylene optionally interrupted by O, N or S and optionally substituted by lower alkyl, lower aralkyl, lower carboxylic acyl, carboxy, protected carboxy; hydroxy, lower alkoxy, lower acyloxy, oxo; amino, lower alkylamino, lower acylamino, nitro, nitroso, lower alkylthio, lower sulfonic acyl or halogen;and the remaining R or P is hydrogen or halogen;and dotted line represents the presence of one or two double bonds).Type: GrantFiled: March 5, 1980Date of Patent: March 19, 1985Assignee: Shionogi & Co., Ltd.Inventor: Makiko Sakai
-
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
-
Patent number: 4501890Abstract: Trans-(.+-.)-2-Amino or substituted amino-4-permissibly-substituted 6-lower alkyl or allyl-5,5a,-6,7,8,9,9a,10-octahydropyrimido[4,5-g]quinolines, the corresponding trans-(-)-stereoisomers and salts thereof, useful in treating anxiety, Parkinson's Syndrome, sexual dysfunction, depression, hypertension and elevated prolactin levels, and intermediates useful for the synthesis thereof.Type: GrantFiled: September 26, 1983Date of Patent: February 26, 1985Assignee: Eli Lilly and CompanyInventors: Cynthia L. Nichols, Edmund C. Kornfeld
-
Patent number: 4500713Abstract: (3S)-2-N-[(1S)-1-Ethoxycarbonyl-1-(2,3-dihydro-1H-inden-2-yl)-methyl]-L-ala nyl-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid is a antihypertensive agent.Type: GrantFiled: September 23, 1982Date of Patent: February 19, 1985Assignee: USV Pharmaceutical CorporationInventors: John T. Suh, Jeffrey N. Barton, John R. Regan
-
Patent number: 4500341Abstract: Phenoxycarboxylic acid amide compound of the formula ##STR1## wherein R.sup.1 and R.sup.2 are individually selected from hydrogen and methyl,R.sup.3 is hydrogen or alkyl with from 1 to 5 carbon atomsR.sup.4 is optionally substituted alkoxycarbonylalkyl, aminocarbonylalkyl or dialkylaminocarbonylalkyl, phenyl, or substituted phenyl wherein the substituent is at least one of the group consisting of alkyl, alkoxy or alkylthio of from 1 to 4 carbon atoms, carbalkoxy of from 2 to 4 carbon atoms, halogen, and nitro; orR.sup.3 and R.sup.Type: GrantFiled: October 21, 1981Date of Patent: February 19, 1985Assignee: Bayer AktiengesellschaftInventors: Heinz Forster, Ludwig Eue, Robert R. Schmidt
-
Patent number: 4499079Abstract: Peptides of the formula ##STR1## wherein X is various amino or imino acids or esters are useful as hypotensive agents.Type: GrantFiled: November 18, 1982Date of Patent: February 12, 1985Assignee: E. R. Squibb & Sons, Inc.Inventors: Eric M. Gordon, Harold N. Weller, III