Three Or More Ring Hetero Atoms In The Tetracyclo Ring System Patents (Class 544/247)
  • Patent number: 4269836
    Abstract: New 4H-pyrazolo[4',3':5,6]pyrido[3,4-e][1,2,4]triazolo[1,5-a]pyrimidin-5(8H)on e and new derivatives thereof have the general formula ##STR1## The compounds are useful as anti-inflammatory agents and central nervous system depressants.
    Type: Grant
    Filed: July 13, 1976
    Date of Patent: May 26, 1981
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Theodor Denzel, Hans Hoehn
  • Patent number: 4255573
    Abstract: Pharmaceutical composition for chelating excess iron in a mammal and facilitating the removal of excess iron from the mammalian body are disclosed which comprise as active ingredient an iron-chelating agent selected from the group consisting of 5H-pyrimido(2',1':2,3)imidazo(4,5-b)indole having the formula ##STR1## 5H-pyrido(2',1':2,3)imidazo(4,5-b) indole having the formula ##STR2## or lower alkyl and/or halogen substituted derivatives thereof and pharmaceutically acceptable acid addition salts thereof. Furthermore the preparation of novel 5H-pyrimido(2',1':2,3)imidazo(4,5-b)indoles and intermediates thereof are disclosed.
    Type: Grant
    Filed: March 29, 1979
    Date of Patent: March 10, 1981
    Inventor: Parimal K. Adhikary
  • Patent number: 4247699
    Abstract: The reaction of isatoic anhydrides with malononitrile in a reaction-inert solvent in the presence of a base to produce 2-amino-3-cyano-4-hydroxy-quinolines and 2-amino-.alpha.,.alpha.-dicyanoacetophenones which are then hydrolyzed and decarboxylated under acid or base conditions to produce 2-amino-4-hydroxy-quinolines, useful as intermediates for preparation of 1-oxo-1H-6-alkoxy-pyrimido[1,2-a]quinoline-2-carboxylic acids and esters of value as antiallergy agents.
    Type: Grant
    Filed: March 14, 1979
    Date of Patent: January 27, 1981
    Assignee: Pfizer Inc.
    Inventor: Saul B. Kadin
  • Patent number: 4235802
    Abstract: Propenimidates are provided having the formula: ##STR1## wherein X and Y are independently O or S; andR.sup.1 and R.sup.2 are independently C.sub.1 -C.sub.4 alkyl, (CH.sub.2).sub.n OR.sup.3 where R.sup.3 is C.sub.1 -C.sub.4 alkyl and n is 1 or 2, CH.sub.2 CH.sub.2 Cl, or CH.sub.2 CF.sub.3, provided that when R.sup.1 or R.sup.2 is CH.sub.2 CH.sub.2 Cl or CH.sub.2 CF.sub.3, then the respective X or Y is O.Preferred propenimidates have X and Y as O and R.sup.1 and R.sup.2 as methyl or ethyl.The propenimidates are made by preparing a monohydrohalide salt from a dihydrohalide salt of the formula: ##STR2## and then contacting the monohydrohalide salt with cyanamide. The propenimidates upon heating ring close to pyrimidines which are useful in preparing herbicidal compounds.
    Type: Grant
    Filed: August 14, 1979
    Date of Patent: November 25, 1980
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Julius J. Fuchs
  • Patent number: 4233300
    Abstract: New derivatives of 8H-pyrazolo[1,5-a]pyrazolo[4',3':5,6]pyrido[3,4-e]pyrimidine have the general formula ##STR1## The compounds are useful as anti-inflammatory agents and central nervous system depressants.
    Type: Grant
    Filed: November 13, 1979
    Date of Patent: November 11, 1980
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Theodor Denzel, Hans Hoehn
  • Patent number: 4232024
    Abstract: Anti-allergy novel 1-oxo-1H-pyrimido[6,1-b]benzthiazole derivatives of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 each independently is hydrogen, halogen, hydroxy, nitro, trifluoromethyl, or lower alkyl, alkoxy or alkylthio, orR.sub.2 and R.sub.3 together are alkylenedioxy, andX is hydroxy, alkoxy or tetrazolyl-5-amino,or salts thereof, as well as their production by saponification of ##STR2## or tautomers thereof, followed by acidification.
    Type: Grant
    Filed: February 26, 1979
    Date of Patent: November 4, 1980
    Assignee: Boehringer Mannheim GmbH
    Inventors: Werner Winter, Herman Hindermayr, Egon Roesch, Androniki Roesch, Otto-Henning Wilhelms
  • Patent number: 4202899
    Abstract: New derivatives of 8H-pyrazolo[1,5-a]pyrazolo[4',3':5,6]-pyrido[3,4-e]pyrimidine have the general formula ##STR1## The compounds are useful as anti-inflammatory agents and central nervous system depressants.
    Type: Grant
    Filed: April 21, 1976
    Date of Patent: May 13, 1980
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Theodor Denzel, Hans Hoehn
  • Patent number: 4183932
    Abstract: Tricyclic quinazolines of the formula, ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and A are as defined in the specification, such as 4,5-dihydro-5-arylimidazo[1,2-a]quinazolines, 4,5-dihydro-5-aryl-s-triazolo[4,3-a]quinazolines and 4,5-dihydro-5-aryltetrazolo[1,5-a]quinazolines having anti-inflammatory and analgesic activity are, for example, prepared by reducing the corresponding 4,5-unsaturated compounds, and then, if necessary, by alkylating the thus produced compounds.
    Type: Grant
    Filed: January 31, 1978
    Date of Patent: January 15, 1980
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Michihiro Yamamoto, Masao Koshiba, Hisao Yamamoto
  • Patent number: 4179560
    Abstract: Imidazo- and pyrimido[2,1-b]quinazolines of the formula, ##STR1## wherein R.sub.1 and R.sub.2 are independently hydrogen, halogen, trifluoromethyl, nitro, C.sub.1-4 alkyl or C.sub.1-4 alkoxy, or R.sub.1 and R.sub.2 may together represent methylenedioxy; R.sub.3 is hydrogen, C.sub.1-4 alkyl, phenyl or substituted phenyl of the formula, ##STR2## (wherein R is halogen, C.sub.1-4 alkyl or C.sub.1-4 alkoxy); R.sub.4 is hydrogen, C.sub.1-4 alkyl or aralkyl; and A is C.sub.2-3 alkylene wich may be optionally substituted by one or two C.sub.1-2 alkyl radicals, and pharmaceutically acceptable acid addition salts thereof, are prepared by reacting a compound of the formula, ##STR3## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and A are as defined above; and X is oxygen or sulfur, with a halogenating agent at a temperature of about 30.degree. C. to about 180.degree. C. In the above imidaxo- and pyrimido[2,1-b]quinazolines, those having C.sub.1-4 alkyl, or ##STR4## as R.sub.
    Type: Grant
    Filed: February 27, 1975
    Date of Patent: December 18, 1979
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Michihiro Yamamoto, Shigeaki Morooka, Masao Koshiba, Shigeho Inaba, Hisao Yamamoto
  • Patent number: 4174397
    Abstract: Thiazolidine derivatives of the formula I ##STR1## in which the substituents R.sup.1 to R.sup.7 have the meanings as indicated in the following and which have in the free form or in the form of their non toxic acid addition salts valuable pharmaceutical properties, processes for preparing them, pharmaceutical preparations on the basis of these compounds and their use as medicines.
    Type: Grant
    Filed: September 6, 1977
    Date of Patent: November 13, 1979
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Bernd Knabe, Hans-Jochen Lang, Ernold Granzer
  • Patent number: 4167569
    Abstract: The invention concerns 3,4-dihydropyrimido [1,2-a]benzimidazole derivatives bearing one or more substituents at positions 6, 7, 8 or 9; processes for their preparation and manufacture; and pharmaceutical compositions thereof. The compounds inhibit the aggregation of blood-platelets and may be used in vivo, in the treatment or prophylaxis of thrombosis or occlusive vascular disease, or in vitro, in helping to stabilize preparations of blood platelets. Representative compounds of the invention are 7- and 8- acetyl-3,4-dihydropyrimido[1,2-a]benzimidazol-2(1H)-one.
    Type: Grant
    Filed: November 23, 1977
    Date of Patent: September 11, 1979
    Assignee: Imperial Chemical Industries Limited
    Inventor: Stuart D. Mills
  • Patent number: 4141979
    Abstract: A series of tetrazolo[a]quinazol-5-ones, methods for their production and use as antiallergy agents and antiulcer agents.
    Type: Grant
    Filed: December 22, 1977
    Date of Patent: February 27, 1979
    Assignee: Pfizer Inc.
    Inventor: Jasjit S. Bindra
  • Patent number: 4134981
    Abstract: Fused heterocyclic ring systems in which a quinoline or a pyridine component is "fused" to a pyrimidine having a 2-methyl, 2-ethyl, or 2-acetyl group and a 4-keto group, and to similar ring systems in which a quinoline, a naphthalene or a pyridine component is "fused" to a pyrimidine having a 2-carboxy group and a 4-keto group, derivatives, and pharmaceutically-acceptable cationic salts thereof, and their use as antiallergy agents, and intermediates therefor.
    Type: Grant
    Filed: October 27, 1977
    Date of Patent: January 16, 1979
    Assignee: Pfizer Inc.
    Inventors: Thomas H. Althuis, Leonard J. Czuba, Hans-Jurgen E. Hess, Saul B. Kadin
  • Patent number: 4128645
    Abstract: New 4H-pyrazolo[1,5-a]pyrazolo[4',3':5,6]pyrido[3,4-e]pyrimidin-5(8H)one and new derivatives thereof have the general formula ##STR1## The compounds are useful as anti-inflammatory agents and central nervous system depressants.
    Type: Grant
    Filed: September 1, 1977
    Date of Patent: December 5, 1978
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Theodor Denzel, Hans Hoehn
  • Patent number: 4127655
    Abstract: New derivatives of 8H-pyrazolo[4',3':5,6]pyrido[3,4-e]-[1,2,4]triazolo[1,5-a]pyrimidine have the general formula ##STR1## The compounds are useful as anti-inflammatory agents and central nervous system depressants.
    Type: Grant
    Filed: January 9, 1978
    Date of Patent: November 28, 1978
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Theodor Denzel, Hans Hoehn
  • Patent number: 4127720
    Abstract: A series of novel pyrimido[2,1-a]isoquinoline derivatives is provided for use as inhibitors of allergic reactions. The compounds exhibit antiallergy activity by both oral and parenteral routes of administration.
    Type: Grant
    Filed: September 21, 1977
    Date of Patent: November 28, 1978
    Assignee: Bristol-Myers Company
    Inventors: Peter F. Juby, Thomas W. Hudyma, Richard A. Partyka
  • Patent number: 4127657
    Abstract: New 4H-pyrazolo[1,5-a]pyrazolo[4',4':5,6]pyrido[3,4-e]pyrimidin-5(8H)one and new derivatives thereof have the general formula ##STR1## The compounds are useful as anti-inflammatory agents and central nervous system depressants.
    Type: Grant
    Filed: September 1, 1977
    Date of Patent: November 28, 1978
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Theodor Denzel, Hans Hoehn
  • Patent number: 4110454
    Abstract: New derivatives of 8H-pyrazolo[4',3':5,6]pyrido[3,4-e][1,2,4]triazolo[1,5-a]pyrimidine have the general formula ##STR1## The compounds are useful as anti-inflammatory agents and central nervous system depressants.
    Type: Grant
    Filed: January 9, 1978
    Date of Patent: August 29, 1978
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Theodor Denzel, Hans Hoehn