Patents Examined by David E. Wheeler
  • Patent number: 3978067
    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
  • Patent number: 3978065
    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
  • Patent number: 3978050
    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.
    Type: Grant
    Filed: January 24, 1975
    Date of Patent: August 31, 1976
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Uwe D. Treuner, Hermann Breuer
  • Patent number: 3976661
    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
  • Patent number: 3976650
    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.
    Type: Grant
    Filed: November 4, 1975
    Date of Patent: August 24, 1976
    Assignee: Pfizer Inc.
    Inventor: Michael R. Johnson
  • Patent number: 3976651
    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.
    Type: Grant
    Filed: April 14, 1975
    Date of Patent: August 24, 1976
    Assignee: Riker Laboratories, Inc.
    Inventors: John F. Gerster, Charles M. Leir
  • Patent number: 3972884
    Abstract: New 14a-aza-D-homo-cholestane derivatives are useful as antifungal agents.
    Type: Grant
    Filed: September 6, 1974
    Date of Patent: August 3, 1976
    Assignee: Eli Lilly and Company
    Inventor: Charles D. Jones
  • Patent number: 3971783
    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
  • Patent number: 3971789
    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
  • Patent number: 3971787
    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
  • Patent number: 3969463
    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.
    Type: Grant
    Filed: January 22, 1975
    Date of Patent: July 13, 1976
    Assignee: Riker Laboratories, Inc.
    Inventor: John F. Gerster
  • Patent number: 3968108
    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.
    Type: Grant
    Filed: March 27, 1974
    Date of Patent: July 6, 1976
    Assignee: Eli Lilly and Company
    Inventors: Stjepan P. Kukolja, Steven R. Lammert
  • Patent number: 3966743
    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
  • Patent number: 3966718
    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
  • Patent number: 3966735
    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
  • Patent number: 3966745
    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
  • Patent number: 3966731
    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.
    Type: Grant
    Filed: September 30, 1974
    Date of Patent: June 29, 1976
    Assignee: Tanabe Seiyaku Co., Ltd.
    Inventors: Ichizo Inoue, Toyonari Oine, Yoshihisa Yamada, Junichi Tani, Ryuichi Ishida, Takashi Ochiai
  • Patent number: 3965102
    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
  • Patent number: 3963746
    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.
    Type: Grant
    Filed: April 28, 1975
    Date of Patent: June 15, 1976
    Assignee: Sterling Drug Inc.
    Inventor: Denis M. Bailey
  • Patent number: 3963724
    Abstract: Various intermediates useful in the preparation of 4-aryl-2,3,3a,4,5,6,7,8,9,9b-decahydro-1H-pyrrolo[3,4-f]quinolines are disclosed.
    Type: Grant
    Filed: February 13, 1975
    Date of Patent: June 15, 1976
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Frederic Peter Hauck, Joseph E. Sundeen