Three Or More Ring Hetero Atoms In The Bicyclo Ring System Patents (Class 544/48)
  • Patent number: 4485107
    Abstract: Novel [[bis(aryl)methylene]-1-piperidinyl]alkyl-pyrimidinones, wherein the pyrimidinone-ring is embraced within a bicyclic system, being useful compounds in the treatment of psychosomatic disorders.
    Type: Grant
    Filed: July 27, 1983
    Date of Patent: November 27, 1984
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Ludo E. J. Kennis, Jan Vandenberk, Josephus C. Mertens
  • Patent number: 4451650
    Abstract: There are disclosed certain 2H-pyrido[4,3-b][1,4]oxazines and 2H-pyrido[4,3-b][1,4]thiazines which possess biological activity. The compounds have the structure: ##STR1## wherein n has a value of 1,2 or 3; X is oxygen or sulfur; R.sub.1 is a lower alkyl group, e.g., an alkyl group containing up to six carbon atoms such as methyl, ethyl, propyl, butyl, etc.; R.sub.2 is a member selected from the group consisting of hydrogen, alkyl radicals having from about one to about 12 carbon atoms, preferably from about one to about six carbon atoms; alkenyl radicals having from about two to about 15 carbon atoms; preferably from about two to about 10 carbon atoms; cycloalkyl radicals having from about three to about 20 carbon atoms, preferably from about three to about 15 carbon atoms; aryl, aralkyl and alkaryl radicals having from about six to about 20 carbon atoms, preferably from about six to about 15 carbon atoms; a halogen radical, e.g.
    Type: Grant
    Filed: October 26, 1982
    Date of Patent: May 29, 1984
    Assignee: Southern Research Institute
    Inventors: Carroll G. Temple, Jr., John A. Montgomery, Robert D. Elliott, Glynn P. Wheeler
  • Patent number: 4443451
    Abstract: Novel 5H-thiazolo- and 5H-1,3,4-thiadiazolo[3,2-a]pyrimidin-5-one and 3,4-dihydro-2H,6H-pyrimido[2,1-b] [1,3]-thiazin-6-one derivatives, which compounds are useful psychotropic agents.
    Type: Grant
    Filed: April 21, 1982
    Date of Patent: April 17, 1984
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Ludo E. J. Kennis, Josephus C. Mertens
  • Patent number: 4437877
    Abstract: A herbicidal composition which comprises as an active ingredient a compound of the formula: ##STR1## wherein X is a chlorine atom or a bromine atom, Y is --CH.sub.2 --, --S-- or --SO.sub.2 -- and R is a C.sub.1 -C.sub.4 alkyl group, an allyl group or a propargyl group, and an inert carrier.
    Type: Grant
    Filed: June 10, 1982
    Date of Patent: March 20, 1984
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Eiki Nagano, Shunichi Hashimoto, Ryo Yoshida, Hiroshi Matsumoto, Katsuzo Kamoshita
  • Patent number: 4414388
    Abstract: Antiallergy and antiulcer agents having the formula (I), ##STR1## and their pharmaceutically acceptable salts, wherein R.sub.1 and R.sub.2 taken separately are each hydrogen or lower alkyl; and R.sub.1 and R.sub.2 taken together are alkylene of 3-9 carbon atoms or phenylalkylene of 9-11 carbon atoms, with the proviso that the ring so formed is between 5- and 8-membered; acids of the formula (II), ##STR2## wherein R.sub.1 and R.sub.2 are as defined above and R.sub.3 is hydrogen, which are useful as intermediates for compounds of the formula (I), but in many instances also possess the same useful biological activity as do formula I compounds; and intermediates of the formula II wherein R.sub.1 and R.sub.2 are defined as above, and R.sub.3 is alkyl of 1 to 4 carbon atoms, carbalkoxy of 2 to 5 carbon atoms, carbophenoxy or carbobenzoxy, are also described.
    Type: Grant
    Filed: December 14, 1981
    Date of Patent: November 8, 1983
    Assignee: Pfizer Inc.
    Inventor: Saul B. Kadin
  • Patent number: 4394505
    Abstract: Novel 5-fluorouracil derivatives of the following general formula ##STR1## wherein R.sup.1 is hydrogen, C.sub.1 -C.sub.5 alkyl, C.sub.6 -C.sub.10 aryl, C.sub.7 -C.sub.10 aralkyl, C.sub.1 -C.sub.12 alkanoyl, C.sub.2 -C.sub.6 alkoxycarbonyl, C.sub.1 -C.sub.5 alkanoyloxymethyl, carbamoyl or tri-C.sub.1 -C.sub.5 alkylsilyl;R.sup.2 is hydrogen, C.sub.1 -C.sub.5 alkyl, C.sub.6 -C.sub.10 aryl or C.sub.7 -C.sub.10 aralkyl;X is hydrogen, halogen or C.sub.2 -C.sub.6 alkoxycarbonyl;Y is O, NR' (R' is hydrogen or C.sub.1 -C.sub.5 alkyl), S, SO or SO.sub.2 ; andn is an integer of 1-3.which are orally administrable anti-tumor agents.
    Type: Grant
    Filed: April 16, 1982
    Date of Patent: July 19, 1983
    Assignee: Shionogi & Co., Ltd.
    Inventors: Susumu Kamata, Wataru Nagata
  • Patent number: 4376769
    Abstract: Disclosed herein are novel tetrahydro imidazo thiazoles, tetrahydro imidazo thiazines, hexahydro imidazo thiazepines and hexahydro imidazo thiazocines, intermediates for the preparation thereof, methods of using the compounds as anti-inflammatory agents and methods of using an intermediate thereof as anti-secretory agents to relieve the symptoms of gastric distress.
    Type: Grant
    Filed: June 19, 1981
    Date of Patent: March 15, 1983
    Assignee: Schering Corporation
    Inventor: Sherlock Margaret H.
  • Patent number: 4361700
    Abstract: Derivatives of pyridopyrimidinone of the following formulae: ##STR1## wherein Y is C.dbd.S, C.dbd.O, SO.sub.2, or CH.sub.2 ;Z is C--H, N, S or O;R.sub.1 is hydrogen, hydroxyl, halogen, lower alkyl or R.sub.3 ;R.sub.2 is hydrogen, aliphatic hydrocarbon, substituted aliphatic hydrocarbon or carbocyclic aryl-aliphatic hydrocarbon, wherein the substituent of the aliphatic hydrocarbon may be hydroxyl, halogen, alkoxy, carboxylic acid ester, or lower alkyl amine;R.sub.3 is ##STR2## wherein A is carbon, nitrogen, oxygen, or sulfur; R.sub.
    Type: Grant
    Filed: May 20, 1980
    Date of Patent: November 30, 1982
    Assignee: James S. Waldron
    Inventors: William P. Purcell, Richard D. Gilliom, Harlie A. Parish, Jr.
  • Patent number: 4315767
    Abstract: Triazolone herbicides of the formula: ##STR1## where V is hydrogen, fluorine, chlorine, bromine, methyl or OR where R is alkyl of 1-4 carbon atoms;X is hydrogen, fluorine, chlorine, bromine, cyano, methyl, methoxy, or nitro;Y is hydrogen, fluorine, chlorine, bromine, or methyl;n, m is 0, 1, 2, 3 or 4;Q is oxygen or sulfur;Z is oxygen, S(O).sub.p or NR';p is 0, 1 or 2 andR' is alkyl of 1-3 carbon atoms with the provisos that(1) n+m=2, 3, or 4; and(2) if n+m=2 or 4 then Y, X.noteq.Hand when Z is S(O)p, n is 1, 2, 3 or 4.
    Type: Grant
    Filed: December 14, 1979
    Date of Patent: February 16, 1982
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Anthony D. Wolf
  • Patent number: 4187303
    Abstract: Thienothiazine derivatives of the formula ##STR1## wherein A, R.sub.1 and R.sub.2 are as hereinafter set forth, and their tautomers are described. The thienothiazine derivatives are useful as anti-inflammatory, analgesic, antirheumatic and antithrombotic agents.
    Type: Grant
    Filed: August 15, 1978
    Date of Patent: February 5, 1980
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Otto Hromatka, Dieter Binder, Paul Zeller, Rudolf Pfister
  • Patent number: 4181799
    Abstract: The compound 5(6H), 8(8aH)-dioxo-1H,3H-thiazolo[4,3-c] [1,4]thiazine is useful as an inhibitor of Angiotensin I converting enzyme.
    Type: Grant
    Filed: November 13, 1978
    Date of Patent: January 1, 1980
    Assignee: Morton-Norwich Products, Inc.
    Inventor: Ralph L. White, Jr.
  • Patent number: 4180662
    Abstract: Anti-inflammatory, analgesic, anti-rheumatic and anti-thrombotic thienothiazine derivatives having the formula ##STR1## wherein A together with the two carbon atoms forms the group ##STR2## and the dotted line indicates the double bond present in the first and last thieno structures above, R.sup.1 is lower alkyl, R.sup.2 is the radical of an aromatic heterocycle with 1 to 4 hetero atoms optionally substituted by one or two lower alkyl groups, or a phenyl radical optionally substituted by halogen, hydroxy, lower alkyl, trifluoromethyl or lower alkoxy, R.sup.3 is halogen and R.sup.3' is hydrogen or halogen,and pharmaceutically acceptable salts thereof are described.
    Type: Grant
    Filed: August 31, 1978
    Date of Patent: December 25, 1979
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Rudolf Pfister, Paul Zeller, Dieter Binder, Otto Hromatka
  • Patent number: 4179276
    Abstract: This invention relates to novel 2-aryl-1H-imidazo-[5,1-c][1,4]thiazine-1,3(2H)-diones, to agricultural compositions containing them and to the method of use of these compounds as pre- or postemergence herbicides for general control of undesirable vegetation. The invention also includes novel intermediate compounds for making the novel compounds.
    Type: Grant
    Filed: March 27, 1978
    Date of Patent: December 18, 1979
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Jiin-Duey Cheng
  • Patent number: 4119777
    Abstract: A thiazine derivative, which forms a color on contact with an electron accepting material, represented by the formula (II): ##STR1## wherein A.sub.1 and A.sub.2, which may be the same or different, each represents an aryl group or a heterocyclic group and A.sub.1 and A.sub.2 may combine together to form a heterocyclic ring or a fluorene ring, the ring B represents an aromatic hydrocarbon ring or a heterocyclic ring, and Y represents a hydrogen atom, an aliphatic group, an aryl group, a heterocyclic group, an amino group, an amido group, an oxy group or a thio group, but at least one of A.sub.1 and A.sub.2 or the ring formed by the combination of A.sub.1 and A.sub.2 represents an electron donating aryl group or an electron donating heterocyclic group, and a process for preparing the thiazine derivatives represented by the formula (II) by oxidizing a thioamide derivative represented by the formula (I): ##STR2## wherein A.sub.1, A.sub.2, B and Y are as above described.
    Type: Grant
    Filed: December 17, 1976
    Date of Patent: October 10, 1978
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Hideo Usui, Sadao Ishige, Keiso Saeki
  • Patent number: 4090020
    Abstract: Thienothiazine derivatives of the formula ##STR1## wherein R.sub.1 is lower alkyl; R.sub.2 is an unsubstituted aromatic heterocyclic radical which contains from 1 to 4 hetero atoms or one which is substituted by one or two lower alkyl groups, or is an unsubstituted phenyl radical or one substituted by halogen, hydroxy, lower alkyl, nitro, trifluoromethyl or lower alkoxy; and R.sub.3 and R.sub.4, independently, are hydrogen or lower alkyl,Prepared inter alia, from novel intermediates, are described. The end products are useful as anti-inflammatory, analgesic and anti-rheumatic agents.
    Type: Grant
    Filed: February 9, 1977
    Date of Patent: May 16, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Dieter Binder, Otto Hromatka, Rudolf Pfister, Paul Zeller
  • Patent number: 4076709
    Abstract: The present invention relates to compounds of the formula ##STR1## wherein A together with the two carbon atoms to which it is attached forms the group ##STR2## AND THE BROKEN LINE REPRESENTS THE DOUBLE BOND IN GROUP (A); R.sub.1 represents a lower alkyl group; R.sub.2 represents the residue of an aromatic heterocyclic ring containing from 1 to 4 hetero atoms, which may be substituted by one or two lower alkyl groups, or a phenyl group which may be substituted by halogen, hydroxy, lower alkyl, trifluoromethyl or lower alkoxy and R.sub.3 and R.sub.4 each represent a hydrogen atom or a lower alkyl group.Also provided are methods for their preparation. The thienothiazine derivatives provided by this invention have anti-flammatory, analgesic and antirheumatic activity.
    Type: Grant
    Filed: August 21, 1975
    Date of Patent: February 28, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Otto Hromatka, Dieter Binder, Rudolf Pfister, Paul Zeller