Three Or More Ring Hetero Atoms In The Bicyclo Ring System Patents (Class 544/91)
  • Patent number: 4723987
    Abstract: Sulfonamides such as N-[(4,6-dimethoxypyrimidin-2-yl)aminocarbonyl]-1,3-dihydro-6-methyl-3-oxof uro[3,4-c]pyridine-4-sulfonamide are useful as herbicides and plant growth regulants.
    Type: Grant
    Filed: April 22, 1986
    Date of Patent: February 9, 1988
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Mary A. Hanagan
  • Patent number: 4703120
    Abstract: The synthesis of furo[3,4-d]pyrimidine-2,4-dione derivatives and their urea intermediates is described. The novel urea intermediates and furo[3,4-d]pyrimidine-2,4-dione derivatives are general vasodilating agents and anti-hypertensive agents. The compounds are useful as cardiovascular agents.
    Type: Grant
    Filed: April 28, 1986
    Date of Patent: October 27, 1987
    Assignee: Ortho Pharmaceutical Corporation
    Inventor: Jeffery B. Press
  • Patent number: 4672063
    Abstract: 5-alkyl-1-phenyl-2-piperazinoalkylpyrazolin-3-one compounds of the Formula ##STR1## in which R.sub.1 is a straight-chain, branched or cyclic alkyl group with up to 6 carbon atoms, Z is an alkylene chain with 2 to 4 carbon atoms, and 1-phenyl substituent is an optionally substituted phenyl ring, and R.sub.4 is a phenyl or pyridyl group which is optionally substituted and their preparation are described. The compounds have pharmacological, particularly antiallergic, properties.
    Type: Grant
    Filed: November 21, 1985
    Date of Patent: June 9, 1987
    Assignee: Kali-Chemie Pharma GmbH
    Inventors: Daniel Jasserand, Marie-Odile Christen, Dominique Biard, Dimitri Yavordios
  • Patent number: 4593093
    Abstract: There are presented compounds of the formula ##STR1## wherein R.sup.1 is one of the 3-substituents usable in cephalosporin chemistry, R.sup.2 is hydrogen, lower alkyl or COOR.sup.3 -lower alkyl, wherein R.sup.3 is hydrogen, a cation of a base or a readily hydrolyzable ester group, and X is sulphur, oxygen or one of the groups --SO-- and --SO.sub.2 --,and the readily hydrolyzable esters, readily hydrolyzable ethers and salts of these compounds and hydrates of the compounds of formula I or of their esters, ethers and salts, also presented are methods for the manufacture of these compounds as well as compounds used in their manufacture.
    Type: Grant
    Filed: April 16, 1984
    Date of Patent: June 3, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Roland Reiner, Urs Weiss
  • Patent number: 4585772
    Abstract: The invention relates to pharmaceutical compositions containing active ingredients of Formula (I) and methods for the use of said compositions to treat cardiac insufficiencies. Also included in the invention are methods of the manufacture of said active ingredients of Formula (I). The invention includes, additionally, compounds of Formula (I).
    Type: Grant
    Filed: July 11, 1983
    Date of Patent: April 29, 1986
    Assignee: Bayer Aktiengesellschaft
    Inventors: Bodo Junge, Siegfried Goldmann, Gunter Thomas, Bernward Garthoff
  • Patent number: 4515944
    Abstract: Intermediates of the isomeric formulae II or III ##STR1## wherein R.sub.1 is a hydrogen or halogen atom, or a lower alkyl, lower alkoxy, hydroxyl, trifluoromethyl or lower alkanoyloxy group,R.sub.2 is a hydrogen or halogen atom, or a lower alkyl or lower alkoxy group, orR.sub.1 and R.sub.2 are bonded to adjacent carbon atoms and together denote a methylenedioxy or ethylenedioxy group,R.sub.3 is a hydrogen or halogen atom, or a lower alkyl, lower alkoxy, hydroxy, trifluoromethyl or lower alkanoyloxy group,R.sub.4 is a hydrogen or halogen atom, or a lower alkyl or lower alkoxy group, orR.sub.3 and R.sub.4 are bonded to adjacent carbon atoms and together denote a methylenedioxy or ethylenedioxy group, Z is an alkylene group with 2 to 6 carbon atoms, Z' is an alkylene group with 2 to 4 carbon atoms, Y is a halogen atom, and Y' is a halogen atom, and acid addition salts thereof, are useful to prepare antiallergic 2-piperazinoalkyl-1, 5-diphenylpyrazolin-3-ones.
    Type: Grant
    Filed: December 22, 1983
    Date of Patent: May 7, 1985
    Assignee: Kali-Chemie Pharma GmbH
    Inventors: Henning Heinemann, Daniel Jasserand, Wolfgang Milkowski, Dimitri Yavordios, Horst Zeugner
  • 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: 4255568
    Abstract: The disclosed 2H-pyrimido[4,5-d][1,3]oxazine-2,4(1H)-dione derivatives are intermediates useful in the production of 7,8-dihydro-2,5,8-trisubstituted-7-oxo-pyrido[2,3-d]pyrimidine-6-carboxyli c acid derivatives which are gastric anti-secretory agents and anti-allergic agents.
    Type: Grant
    Filed: October 29, 1979
    Date of Patent: March 10, 1981
    Assignee: American Home Products Corporation
    Inventors: Anthony C. Scotese, Robert L. Morris, Arthur A. Santilli
  • Patent number: 4252804
    Abstract: Compounds of the formula I ##STR1## wherein m and n are 0, 1 or 2, X represents oxygen, imino, benzylimino, or morpholinoethylimino, Y represents CO, CONH, COO or SO.sub.2, and NR.sub.1 R.sub.2 represents a dimethylamino, diethylamino, dipropylamino, dibutylamino, allylamino, isobutenylamino, cyclopentylamino, cyclohexylamino, cycloheptylamino, cyclooctylamino, N-methyl N-cyclopentylamino, N-methyl N-cyclohexylamino, N-allyl N-cyclohexylamino, adamantylamino, diethoxyethylamino, dimethylaminoethylamino, dimethylaminopropylamino, N-methyl N-dimethylaminopropyl-amino, benzylamino, 3,4,5-trimethoxybenzylamino, phenethylamino, p-chlorophenethylamino, tetrahydrofurfurylamino, tetrahydropyranylmethylamino, pyrrolidino, isoxazolidinyl, piperidino, 4-hydroxypiperidino, 4-m-chlorophenyl-4-hydroxypiperidino, homopiperidino, 1,2,3,6-tetrahydropyridyl, morpholino, 2-methylmorpholino, 2,6-dimethylmorpholino, 2-morpholinoethylamino, thiamorpholino, piperazino, 4-methylpiperazino, 4-(.alpha.
    Type: Grant
    Filed: January 13, 1978
    Date of Patent: February 24, 1981
    Assignee: Metabio-Joullie
    Inventors: Maurice Joullie, Gabriel Maillard, Lucien Lakah, Christian J. M. Warolin
  • Patent number: 4234581
    Abstract: 2-Aminothiophene-3-carboxamides are converted to oxamates or fumaramides by acylation of the amino group. Cyclization yields thieno[2,3-d]pyrimidines which may also be prepared from the corresponding oxazines. Compounds illustrative of those having inhibitory action on the immediate hypersensitivity reaction in mammals are N-[3-(aminocarbonyl)-4,5,6,7-tetrahydrobenzo[b]thien-2-yl]oxamic acid, ethyl 5,6,7,8-tetrahydro-4-oxo-4H-benzothieno[2,3-d][1,3]oxazine-2-carboxylate, and ethyl 3,4-dihydro-6-ethyl-4-oxothieno[2,3-d]pyrimidine-2-carboxylate.
    Type: Grant
    Filed: March 30, 1979
    Date of Patent: November 18, 1980
    Assignee: Mead Johnson & Company
    Inventor: Davis L. Temple, Jr.
  • Patent number: 4159377
    Abstract: 2-Aminothiophene-3-carboxamides are converted to oxamates or fumaramides by acylation of the amino group. Cyclization yields thieno[2,3-d]pyrimidines which may also be prepared from the corresponding oxazines. Compounds illustrative of those having inhibitory action on the immediate hypersensitivity reaction in mammals are N-[3-(aminocarbonyl)-4,5,6,7-tetrahydrobenzo[b]thien-2-yl]oxamic acid, ethyl 5,6,7,8-tetrahydro-4-oxo-4H-benzothieno[2,3-d][1,3]oxazine-2-carboxylate, and ethyl 3,4-dihydro-6-ethyl-4-oxothieno[2,3-d]pyrimidine-2-carboxylate.
    Type: Grant
    Filed: August 22, 1977
    Date of Patent: June 26, 1979
    Assignee: Mead Johnson & Company
    Inventor: Davis L. Temple, Jr.
  • Patent number: 4152427
    Abstract: Substituted pyrimidinone [(di)-thio]-phosphoric(phosphonic) acid esters and ester-amides of the formula ##STR1## IN WHICH R represents alkyl,R.sup.1 represents alkyl, phenyl, alkoxy, alkylthio or alkylamino,X represents oxygen or sulphur,Y represents oxygen or alkylamino, andN represents 2, 3, or 4,Which possess arthropodicidal and nematicidal properties.
    Type: Grant
    Filed: January 5, 1978
    Date of Patent: May 1, 1979
    Assignee: Bayer Aktiengesellschaft
    Inventors: Fritz Maurer, Ingeborg Hammann, Bernhard Homeyer
  • Patent number: 4054653
    Abstract: Substituted pyrido[3,4-e]oxazine diones, e.g., 6-methyl-4,7-diphenyl-2H-pyrido[3,4-e]-1,3-oxazine-2,5-dione are useful as minor tranquilizers, sleep inducers and muscle relaxants.
    Type: Grant
    Filed: June 1, 1976
    Date of Patent: October 18, 1977
    Assignee: Sandoz, Inc.
    Inventor: Jeffrey Nadelson