Abstract: Novel 2-substituted-5,6-dimethoxyindazoles of the formula: ##STR1## where R is cyclohexyl, phenethyl, phenyl, dimethylamino, aminoalkyl, methoxyethyl, indazolylethyl, tetrahydropyranylmethyl, p-dimethylaminophenyl, 2-hydroxyethyl, allyl, thiazolyl, pyridyl, 2,3-dihydroxypropyl, and hydroxy are useful as central nervous system depressants or hypotensive agents.
Type:
Grant
Filed:
February 25, 1976
Date of Patent:
March 29, 1977
Assignee:
Morton-Norwich Products, Inc.
Inventors:
Thomas J. Schwan, Charles S. Davis, LeRoy J. Honkomp
Abstract: Compounds of the class of spiro[norbornane-2,3'-piperidines], spiro[bicyclo[2.2.2]octane-2,3'-piperidines], and corresponding spiro-pyrrolidine derivatives which are unsubstituted at the ring nitrogen atom or substituted by neutral or basic radicals, and the pharmaceutically acceptable acid addition salts of these new compounds possess valuable pharmacological properties and are active ingredients for pharmaceutical compositions. In particular, these new compounds have an antiviral activity. Specific embodiments are (1RS,2RS,4SR)-spiro[norbornane-2,3'-piperidine]-hydrochloride and 1'-[2-(2-azaspiro[5.5]undec-2-yl)-ethyl]-spiro[bicyclo[2.2.2]octane-2,3'-p iperidine]-dihydrochloride.
Type:
Grant
Filed:
July 23, 1975
Date of Patent:
March 29, 1977
Assignee:
Ciba-Geigy Corporation
Inventors:
Karl Schaffner, Alex Meisels, Jean Claude Roger, Claus D. Weis
Abstract: This invention encompasses novel 5-[1,1-diphenyl-3-(5-or 6-hydroxy-2-azabicyclo[2.2.2]oct-2-yl)propyl]-2-alkyl-1,3,4-oxadiazoles and their lower O-alkanoyl derivatives. These compounds are useful anti-diarrheal agents and also possess little or no analgesic activity.
Type:
Grant
Filed:
March 10, 1976
Date of Patent:
March 22, 1977
Assignee:
G. D. Searle & Co.
Inventors:
Gilbert W. Adelstein, Aziz Karim, Chung H. Yen
Abstract: This invention encompasses novel 2,2-diaryl-3-(1-azabicyclo[2.2.2]oct-2-yl)propionamides and intermediates thereto. These compounds are useful anti-diarrheal agents which possess little or no analgesic activity.
Abstract: This invention relates to substituted indolobenzoxazepines which act as central nervous system depressants and as such are useful as tranquillizers.
Abstract: This invention encompasses novel 2-[5-(cyclic amino)ethyl-10,11-dihydro-5H-dibenzo[a,d] cyclohepten-5-yl]-5-alkyl-1,3,4-oxadiazoles and congeners, useful as anti-diarrheal agents.
Abstract: 3-Indolyl pyridyl ketones of the general formula: ##STR1## and pharmaceutically acceptable acid addition salts thereof wherein R.sub.1 representsA straight- or branched-chain saturated or unsaturated alkyl group having not more than 6 carbon atoms, a benzyl group optionally substituted in the aromatic portion by a chlorine atom or a methoxy groupOr ##STR2## wherein A represents an alkylene chain of from 2 to 6 carbon atoms and R.sub.4 and R.sub.5, which may be the same or different, are each an alkyl group having from 1 to 5 carbon atoms, or R.sub.4 and R.sub.5 are joined together to form with the nitrogen atom a piperidino, pyrrolidino or morpholino group,R.sub.2 representsA branched-or straight-chain alkyl group having from 1 to 4 carbon atoms, a phenyl group optionally substituted by a fluorine, chlorine, or bromine atom or a methoxy or cyclohexyl group; andR.sub.3 representsA 2-pyridyl, 3-pyridyl or 4-pyridyl group.They are effective as fibrinolytic and anti-inflammatory agents.
Abstract: The invention relates to a compound of formula I ##STR1## or pharmaceutically acceptable acid addition salts thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are the same or different and represent hydrogen, or lower alkyl, and R.sup.6 represents hydrogen, alkyl or 1 to 3 carbon atoms, which may be substituted by diloweralkylamino; lower alkanoyl or aroyl.The compounds are either anti-ulcer agents or intermediates for such compounds.
Abstract: The invention provides compounds of formula ##STR1## wherein A and B are hydrogen and R is hydrogen or cycloalkyl, or A and B together form an additional bond and R is cycloalkyl or cycloalkyl-alkyl. Useful in treating pathological disturbancies involving an anoxia factor.
Type:
Grant
Filed:
June 23, 1975
Date of Patent:
March 8, 1977
Assignee:
Synthelabo
Inventors:
Don Pierre Rene Lucien Giudicelli, Henry Najer, Patrick Andre Louis Lardenois, Jean Pierre Gaston Lefevre, Bogdan Iliesco-Branceni, Icilio Angelo Girolamo Cavero
Abstract: 1-(2-Substituted-hydrazino)-3,4-dihydroisoquinolines, prepared in one process by alkylating the corresponding 3,4-dihydroisocarbostyrils, hydrazinolyzing the resulting 1-alkoxy-3,4-dihydroisoquinolines and condensing the resulting 1-hydrazIno-3,4-dihydroisoquinolines with aldehydes or ketones, and 1,1'-azinobis(1,2,3,4-tetrahydroisoquinolines), prepared by condensing corresponding 1-alkoxy-3,4-dihydroisoquinolines and 1-hydrazino-3,4-dihydroisoquinolines, are useful as antihypertensive agents and/or as antiinflammatory agents.
Abstract: 11-Oxygenated-2,6-methano-3-benzazocines N-alkylated by alkylmethyl, haloalkenylmethyl, alkynylmethyl, cycloalkylmethyl, cycloalkenylmethyl, cycloalkyl or 2-cycloalkenyl are prepared directly by N-alkylation of the corresponding N-H intermediates or indirectly by N-acylation of the corresponding N-H intermediates followed by reduction of the resulting N-acylated intermediates and are useful as antagonists of narcotic analgesics.
Abstract: A novel procedure for the preparation of biotin, using cysteine as the starting material is disclosed. This process results in the obtention of pure d-biotin thus obviating the need for a chemical resolution. Novel intermediates are also disclosed.
Type:
Grant
Filed:
March 18, 1976
Date of Patent:
February 22, 1977
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Enrico Baggiolini, Pasquale Nicholas Confalone, Giacomo Pizzolato, Milan Radoje Uskokovic
Abstract: Novel 2,7-bis basic alkanol derivatives of xanthene and thioxanthene, their preparation and use for the prevention and inhibition of viral infections are disclosed.
Abstract: The invention relates to new 3-substituted 1-alkyl-4-phenylpiperidines, being useful as antidepressant and anti-Parkinson agents, and to their production.
Type:
Grant
Filed:
July 23, 1975
Date of Patent:
February 8, 1977
Assignee:
A/S Ferrosan
Inventors:
Jorgen Anders Christensen, Richard Felt Squires
Abstract: N-acyl-N-norsalutaridines can be made by oxidative coupling of N-acyl-N-norreticulines using thallium tristrifluoroacetate or a coordinating agent and an oxidizing agent. The N-acyl-N-norsalutaridines can be converted to thebaine, N-northebaine, and N-substituted-N-northebaines, which can be converted to opium alkaloids and related compounds.
Abstract: Compounds having the structure ##STR1## and pharmaceutically acceptable salts thereof, wherein Z is oxygen, sulfur or methylene; R.sub.1 is hydrogen, halogen, alkyl, aryl or arylalkyl; R.sub.2 is hydrogen, alkyl, aryl, or arylalkyl; R.sub.3 is hydrogen, alkyl, aryl or arylalkyl; and R.sub.4 is hydrogen, halogen, alkyl, phenyl, dialkylamidosulfonyl or trifluoromethyl, have useful central nervous system activity.
Abstract: Vincamine and/or its stereoisomers, a known drug, is made from vincaminol and/or its stereoisomers by successive conversion of the latter into apovincaldehyde, apovincamine, and 16-methoxycarbonyl-eburnane, followed by conversion of the last into vincamine either directly by introduction of a 16-hydroxyl group or by hydrolysis, introduction of a 16-hydroxyl group, and re-esterification.
Abstract: Pyridinium, pyridazinium, pyrimidinium, and pyrazinium halides, respectively having an N-(phenacyl) substituent and the corresponding ylids obtained therefrom by alkaline treatment which compounds are useful as herbicides and/or insecticides.