Six-membered Hetero Ring Consists Of Oxygen, Nitrogen And Carbon (e.g., 1,2-oxazines, Etc) Patents (Class 544/63)
  • Patent number: 4115647
    Abstract: A new class of chemical compounds and their process of preparation is described. These compounds have valuable properties as anti-secretory, anti-spasmodic, anti-ulcerogenic and anti-diarrheal agents.
    Type: Grant
    Filed: June 17, 1977
    Date of Patent: September 19, 1978
    Assignee: William H. Rorer, Inc.
    Inventors: George Henry Douglas, William Lyon Studt, Stuart Alan Dodson
  • Patent number: 4109086
    Abstract: Dienylphosphates of the formula ##STR1## wherein each of R.sub.1 and R.sub.1' is lower alkyl, aryl or benzyl and each of R.sub.2, R.sub.3 and R.sub.4 is hydrogen or lower alkyl,Are useful as anthelmintic agents and as intermediates for enolphosphates having anthelmintic activity.
    Type: Grant
    Filed: February 7, 1977
    Date of Patent: August 22, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Kaspar F. Burri, Frank Kienzle, Perry Rosen
  • Patent number: 4082851
    Abstract: The invention relates to a series of new compounds, salts thereof and to methods for the preparation of the compounds which have the general formula ##STR1## in which R.sub.1 stands for an unsubstituted or substituted phenoxy, phenylthio, benzyl, phenylsulfinyl, or anilino radical;R.sub.2 stands for a -YR.sub.2 ' radical, in which Y represents -O-, -S-, or -NH-, and R.sub.2 ' represents C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl or -alkynyl; or methyl or ethyl substituted with phenyl, furyl, thienyl or pyridyl;R.sub.3 and R.sub.4 which can be the same or different, and unsubstituted or substituted, stand for hydrogen or for a straight or branched C.sub.1 -C.sub.8 -alkyl, C.sub.2 -C.sub.8 -alkenyl or -alkynyl radical, a C.sub.5 -C.sub.7 -cycloalkyl, a phenyl, or a 5-, 6- or 7-membered heterocyclic ring system containing not more than two hetero atoms selected from the group consisting of oxygen, sulphur and nitrogen, or for a C.sub.1 -C.sub.
    Type: Grant
    Filed: June 16, 1976
    Date of Patent: April 4, 1978
    Assignee: Leo Pharmaceutical Products Ltd.
    Inventors: Peter Werner Feit, Ole Bent Tvaermose Nielsen, Herta Bruun, Claus Aage Svensgaard Bretting
  • Patent number: 4069256
    Abstract: N-{3-[R.sub.1 -(phenyl)-C(=X)]-phenyl-lower-alkyl}amines having anti-inflammatory utility are prepared either by reduction of a 3-[R.sub.1 -(phenyl)-CO]-phenyl-lower-alkanoylamine; by benzoylating a phenyl-lower-alkylamine; by reaction of a 3-lithiophenyl-lower-alkylamine with a R.sub.1 -(phenyl)-carboxaldehyde, a R.sub.1 -(phenyl)lower-alkyl ketone or a R.sub.1 -(phenyl)-carbonitrile or by transformations involving manipulations of a carbonyl or carbinol group.
    Type: Grant
    Filed: December 17, 1975
    Date of Patent: January 17, 1978
    Assignee: Sterling Drug Inc.
    Inventor: Bernard L. Zenitz
  • Patent number: 4066758
    Abstract: N.sup.2 -naphthalenesulfonyl-L-arginine esters and amides having the formula ##STR1## or the acid addition salts thereof with a pharmaceutically acceptable acid, wherein R is selected from the class consisting of (1) alkoxy, alkenyloxy, cycloalkoxy and halogenated alkoxy, respectively containing not more than 10 carbon atoms, aralkyloxy of not more than 15 carbon atoms, and alkoxy of not more than 10 carbon atoms substitured with an alkoxy group of not more than 10 carbon atoms; ##STR2## wherein R.sub.1 and R.sub.
    Type: Grant
    Filed: March 29, 1976
    Date of Patent: January 3, 1978
    Assignees: Mitsubishi Chemical Industries Limited, Shosuke Okamoto
    Inventors: Shosuke Okamoto, Ryoji Kikumoto, Kazuo Ohkubo, Shinji Tonomura, Yoshikuni Tamao, Tohru Tezuka, Akiko Hijikata
  • Patent number: 4062963
    Abstract: N.sup.2 -naphthalenesulfonyl-L-arginine esters and amides having the formula ##STR1## or the acid addition salts thereof with a pharmaceutically acceptable acid, wherein R is selected from the class consisting of (1) alkoxy, alkenyloxy, cycloalkoxy and halogenated alkoxy, respectively containing not more than 10 carbon atoms, aralkyloxy of not more than 15 carbon atoms, and alkoxy of not more than 10 carbon atoms substituted with an alkoxy group of not more than 10 carbon atoms; ##STR2## wherein R.sub.1 and R.sub.
    Type: Grant
    Filed: March 29, 1976
    Date of Patent: December 13, 1977
    Assignees: Mitsubishi Chemical Industries Limited, Shosuke Okamoto
    Inventors: Shosuke Okamoto, Ryoji Kikumoto, Kazuo Ohkubo, Shinji Tonomura, Yoshikuni Tamao
  • Patent number: 4061642
    Abstract: Compounds of the formula ##STR1## wherein X is aliphatic, cycloaliphatic, aromatic, aralkyl, hetaryl, hetarylalkyl or hydrogen; Y is aliphatic, aromatic, aralkyl, --COOR.sub.1, --COR.sub.2, ##STR2## --SO.sub.2 R.sub.2, ##STR3## --CN, --NH.sub.2, --NO, --NO.sub.2 or hydrogen with the proviso that when Y is hydrogen, X is other than hydrogen; Z.sub.1 is cyano, ##STR4## --NH--OR.sub.10, ##STR5## --OR.sub.12, --SR.sub.12 or --SO.sub.2 R.sub.12 and Z.sub.2 is chlorine, bromine, cyano, hydroxy, mercapto, --OR.sub.12, --SR.sub.12, --SO.sub.2 R.sub.12, ##STR6## --NH--OR.sub.10 or ##STR7## R.sub.1 is aliphatic; R.sub.2 is aliphatic, cycloaliphatic, aromatic, aralkyl or heterocyclic; R.sub.3 and R.sub.4 when taken separately are hydrogen, aliphatic, cycloaliphatic, aromatic or aralkyl; R.sub.3 and R.sub.4 when taken together with the nitrogen atom to which they are attached form a heterocyclic moiety; R.sub.5 and R.sub.6 when taken separately are aliphatic, aromatic, aralkyl, heterocyclic or hydrogen; R.sub.5 and R.
    Type: Grant
    Filed: May 19, 1976
    Date of Patent: December 6, 1977
    Assignee: Cassella Farbwerke Mainkur AG
    Inventors: Erwin Fleckenstein, Ernst Heinrich, Reinhard Mohr
  • Patent number: 4058557
    Abstract: A new class of chemical compounds and their process of preparation is described. These compounds have valuable properties as anti-secretory, anti-spasmodic, anti-ulcerogenic and anti-diarrheal agents.
    Type: Grant
    Filed: March 30, 1976
    Date of Patent: November 15, 1977
    Assignee: William H. Rorer, Inc.
    Inventors: George Henry Douglas, William Lyon Studt, Stuart Alan Dodson
  • Patent number: 4049715
    Abstract: The invention relates to novel 1-(4-R.sub.1 O-phenyl)-2-(4-R.sub.2 -phenyl)-6-R.sub.3 -1,2,3,4-tetrahydroquinolines having anti-fertility and hypocholesterolemic activities, to their preparation, and to novel intermediates therefor.
    Type: Grant
    Filed: July 3, 1975
    Date of Patent: September 20, 1977
    Assignee: Sterling Drug Inc.
    Inventor: Malcolm R. Bell