Abstract: Provided are 5-alkoxy-2-alkyl-7,8-cyclopentano[ h]-1,2,3,4-tetrahydroisoquinoline-1'-ones of the formula ##SPC1##Wherein R and R.sub.1 are the same or different lower alkyl groups, acid addition salts and quaternary ammonium salts thereof, and pharmaceutical compositions containing one or more of the compounds useful as hypotensive agents, and processes of producing the compounds.Also provided are novel 5-alkoxy-2-alkyl-1,2,3,4-tetrahydroisoquinoline intermediates of the formula ##SPC2##Wherein A is CHO-, HOOC-CH=CH-, or HOOC-CH.sub.2 -CH.sub.2 -, R and R.sub.1 are the same or different lower alkyl groups, and acid addition salts and quaternary ammonium salts thereof.
Type:
Grant
Filed:
March 28, 1974
Date of Patent:
August 31, 1976
Assignee:
Marion Laboratories, Inc.
Inventors:
Ian William Mathison, William Ebenezer Solomons, Raymond Henry Jones
Abstract: New reserpine-like compounds of the general formula ##SPC1##Wherein R is a member of the class consisting of hydrogen, lower alkyl, lower alkenyl and acyl; R.sub.1 is selected from hydrogen and lower alkyl, and R.sub.2 is hydrogen or lower alkyl. The new reserpine-like compounds are useful anti-hypertensive agents.
Type:
Grant
Filed:
May 24, 1974
Date of Patent:
August 31, 1976
Assignee:
Gruppo Lepetit S.p.A.
Inventors:
Emilio Occelli, Luigi Fontanella, Giangiacomo Nathansohn
Abstract: 3-Heterothio derivatives of [[(alkoxy)thiocarbonyl]oxy]acetyl cephalosporins having the formula ##EQU1## wherein R is hydrogen, lower alkyl, phenyl-lower alkyl, tri(lower alkyl)stannyl, tri(lower alkyl)silyl, a salt forming ion or the group ##EQU2## R.sub.1 is hydrogen, lower alkyl, phenyl, pyridyl, thienyl or furyl; R.sub.2 is lower alkyl or phenyl-lower alkyl; R.sub.3 is 1-oxopyridinyl or a five membered heterocycle containing only nitrogen and carbon or nitrogen, carbon and oxygen or sulfur in the ring; R.sub.4 is lower alkyl, phenyl or phenyl-lower alkyl; are useful as antibacterial agents.
Abstract: Novel trimethine hemioxonol dyes are provided in which the polymethine chain of the dye includes the 1, 2 and 3 carbon atoms of a 1-cyclohexen-3-ylidene nucleus, the 1-carbon atom of said 1-cyclohexen-3-ylidene nucleus having the nitrogen atom of a tertiary amino group attached thereto. Photographic emulsions and elements are also provided featuring the trimethine hemioxonol dyes of the invention as spectral sensitizers or as filter material.
Type:
Grant
Filed:
January 18, 1974
Date of Patent:
August 24, 1976
Assignee:
Eastman Kodak Company
Inventors:
Leslie G. S. Brooker, Arthur Fumia, Jr., Donald W. Heseltine
Abstract: Process for preparing d(+)-6,7-dimethoxy-2-methyl-4-oxo-1,2,3,4-tetrahydro-1-quinoline carboxylic acid, alkyl or benzyl esters as analgesic agents.
Abstract: Intermediates for and a process for preparing certain substituted 6,7-dihydro-7-hydroxy-1-oxo-1H,5H-benzo[ij]quinolizine carboxylic acids is described. The end products are useful antibacterial agents.
Abstract: Certain novel 7-alkoxy-4-(N-[.omega.-(heteroaryl)alkyl]amino)quinazoline compounds, optionally bearing an alkyl or substituted alkyl group at the 2-position, an alkyl, benzyl, phenyl or alkoxyphenyl group on the 4-amino nitrogen atom, an alkyl or alkoxy group at the 5-position, and an alkyl alkoxy, hydroxy or amino group at the 6-position; and the acid-addition salts thereof. Compounds are cardiac stimulants.
Type:
Grant
Filed:
April 26, 1974
Date of Patent:
July 27, 1976
Assignee:
Pfizer Inc.
Inventors:
Ian Thompson Barnish, David Alexander Cox, Anthony Garth Evans
Abstract: The disclosure describes new 4-aminoquinoline derivatives of general formula ##SPC1##And their acid addition salts, where X is a halogen atom or a trifluoromethyl group, Z is a hydrogen atom or a defined substituent, R is group of the formula--R.sub.3 N--A--NR.sub.1 R.sub.2 (II), ##SPC2##where A in formula II is a chain of 1 to 5 methylene groups which may be substituted with alkyl, the ring in formula IIIa and IIIb is a piperidine or pyrrolidine ring that may be substituted with alkyl and R.sub.1, R.sub.2 and R.sub.3 represent hydrogen or certain defined substituents. The new 4-aminoquinoline derivatives show anti-malarial activity and, in some cases, show one or more of the following activities:- anti-inflammatory activity, anti-hypertensive activity, anti-trichomonal activity, inhibition of blood platelet aggregation, anti-ulcer activity and activity against allergic asthma.
Type:
Grant
Filed:
January 23, 1975
Date of Patent:
July 27, 1976
Assignee:
John Wyeth & Brother Limited
Inventors:
John Leheup Archibald, John Terence Arnott Boyle, John Christopher Saunders
Abstract: 3-(7-Halo-4-quinolyl)-N-[di(loweralkyl)amino(lower alkyl)]-N-(lower alkyl)benzamides and 4-(7-halo-4-quinolyl)-N-[di(lower alkyl)amino(loweralkyl)]-N-(lower alkyl)benzamides and their pharmaceutically acceptable acid addition salts exhibit interesting anti-inflammatory activity. They also exhibit anti-malarial activity and anti-hypertensive activity.
Type:
Grant
Filed:
January 23, 1975
Date of Patent:
July 27, 1976
Assignee:
John Wyeth & Brother Limited
Inventors:
John Leheup Archibald, John Arnott Boyle, John Christopher Saunders
Abstract: Certain substituted 6,7-dihydro-1-oxo-1H,5H-benzo[ij]-quinolizine-2-carboxylic acids and hydrazides, esters, amides and salts thereof, intermediates therefor, and a process for their preparation are described; the compounds are active as anti-microbial agents.
Abstract: A 3.alpha.-methyl-3.beta.-halocepham compound and/or a 2.alpha.-methyl-2.beta.-halomethylpenam compound is converted to a mixture comprising a 3-methyl-3-cephem (desacetoxycephalosporin), a 3.alpha.-methyl-3.beta.-acyloxycepham, and a 2.alpha.-methyl-2.beta.-acyloxymethylpenam by reaction of said 3-halocepham compound and/or said 2-halomethylpenam compound with a silver salt of a lower alkyl carboxylic acid or a cycloalkyl carboxylic acid.
Abstract: Cycloalkano-quinolone derivatives having anti-microbial activity characterized by the formula: ##SPC1##Wherein one of R.sub.1 and R.sub.2 designates hydrogen, halogen, nitro, amino, hydroxyl, acylamino, acyloxy, alkoxy or aryloxy and the other taken together with R.sub.3 forms an akylene bridge containing 2 to 6 carbon atoms, X is hydrogen, lower alkyl, which may be substituted by a member of the group consisting of halogen, hydroxyl, acyloxy, alkoxy, aryloxy, aralkyloxy, mercapto, alkylmercapto, arylmercapto, arylsulfonyl, and alkylsulfonyl, or X is unsubstituted alkenyl including alkadienyl, or alkynyl and Y is hydroxyl, amino or lower alkoxy, and the pharmaceutically acceptable salts thereof.
Type:
Grant
Filed:
September 9, 1974
Date of Patent:
June 29, 1976
Assignee:
Boehringer Mannheim G.m.b.H.
Inventors:
Herbert Berger, Alfred Rhomberg, Kurt Stach, Wolfgang Vomel, Winfriede Sauer
Abstract: Antimicrobially active substituted ceph-3-ems, procedure for their preparation and intermediates for use in the procedure are described. These cephalosporins are characterized by having a 2- or 3- pyridyl group attached to the carbon atom of the methylene group in the 3-position by a carbon-carbon bond and not a carbon-nitrogen bond.
Type:
Grant
Filed:
January 17, 1974
Date of Patent:
June 29, 1976
Assignee:
Beecham Group Limited
Inventors:
Edward George Brain, Neal Frederick Osborne
Abstract: Piperazine derivatives having the following general formula ##EQU1## in which n is 2 or 3, X is an oxy or thio radical, and A and B are each a radical of the group consisting of phenyl radicals containing at most three substituents of the group consisting of nitro, trifluoromethyl, halogen, cyano, and alkyl, alkoxy, alkylthio, acyl, and alkylsulfonyl radicals containing at most 6 carbon atoms, and similar cycloalkyl and cycloalkylalkyl radicals, their acid addition salts, processes for their production, and pharmaceutical compositions containing the same. The compounds have a very favorable action on the central nervous system and are effective agents for the treatment of anxiety states, psychoses, emotional disturbances, aggressive tendencies, and can be used generally for the treatment of psychiatrically disturbed and psychoneurotic patients.
Type:
Grant
Filed:
March 5, 1974
Date of Patent:
June 29, 1976
Assignee:
Kali-Chemie Aktiengesellschaft
Inventors:
Wolfgang Milkowski, Horst Zeugner, Klaus-Wolf VON Eickstedt, Werner Stuhmer
Abstract: Compounds of the general formula ##SPC1##Wherein R.sub.1 is H or OH and R.sub.2 is H or R.sub.1 and R.sub.2 together represent an additional double bond between the two carbon atoms to which they are attached and m and n are integers of 1 to 5 and 2 to 7 respectively; and pharmaceutically acceptable acid addition salts thereof. The compounds are useful for the treatment of vascular disorders in mammals.
Type:
Grant
Filed:
May 6, 1974
Date of Patent:
June 29, 1976
Assignee:
Synthelabo
Inventors:
Don Pierre Rene Lucien Giudicelli, Henry Najer, Bogdan Iliesco-Branceni, Yves Robert Alain Pascal
Abstract: N-(2-amino-5-nitrobenzoyl)-o-toluidine is condensed with fluoroacetic acid or a functional derivative thereof. N-(2-fluoroacetamido-5-nitrobenzoyl)-o-toluidine obtained by said condensation reaction is dehydrated to produce 2-fluoromethyl-3-(o-tolyl)-6-nitro-4(3H)-quniazolinone, which is then subjected to reduction reaction. 2-fluoromethyl-3-(o-tolyl)-6-amino-4(3H)-quinazolinone thus obtained and a pharmaceutically acceptable acid addition salt thereof are useful as central muscle relaxants, minor tranquilizers, anti-convulsants, analgesics and/or anti-inflammatory agents.
Abstract: 1,2,3,4,6,7,8,8a-Octahydro-6-phenyl or substituted phenyl-isoquinolines and derivatives thereof and their methods of preparation are disclosed. These compounds are useful as anti-inflammatory agents.
Type:
Grant
Filed:
October 4, 1974
Date of Patent:
June 22, 1976
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Frederic Peter Hauck, Joseph E. Sundeen
Abstract: 4,5-Dihalopyrrol-2-yl di- and trihalomethyl ketones, prepared by reaction of pyrrole with a di- or trihaloacetyl halide or with a di- or trihaloacetic anhydride and halogenation of the resulting pyrrol-2-yl di- or trihalomethyl ketone, useful as antibacterial, herbicidal and insecticidal agents.