GB1382487A - Substituted pyrido-3,2-d-pyrimidines - Google Patents

Substituted pyrido-3,2-d-pyrimidines

Info

Publication number
GB1382487A
GB1382487A GB1621272A GB1621272A GB1382487A GB 1382487 A GB1382487 A GB 1382487A GB 1621272 A GB1621272 A GB 1621272A GB 1621272 A GB1621272 A GB 1621272A GB 1382487 A GB1382487 A GB 1382487A
Authority
GB
United Kingdom
Prior art keywords
group
compounds
chloro
amino
thiol
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired
Application number
GB1621272A
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Boehringer Ingelheim Pharma GmbH and Co KG
Original Assignee
Dr Karl Thomae GmbH
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from DE19712117657 external-priority patent/DE2117657B2/en
Priority claimed from DE19722202367 external-priority patent/DE2202367A1/en
Priority claimed from DE19722208534 external-priority patent/DE2208534A1/en
Priority claimed from DE19722208535 external-priority patent/DE2208535A1/en
Application filed by Dr Karl Thomae GmbH filed Critical Dr Karl Thomae GmbH
Publication of GB1382487A publication Critical patent/GB1382487A/en
Expired legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/42—One nitrogen atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48—Two nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

1382487 Substituted pyrido-pyrimidine compounds DR KARL THOMAE GmbH 7 April 1972 [10 April 1971 19 Jan 1972 23 Feb 1972 (2)] 16212/72 Heading C2C Novel compounds of the Formula I wherein R 1 and R 2 , which are the same or different, each are morpholino, thiomorpholino, 1-oxidothiomorpholino, 1,1 -dioxidothiomorpholino or piperidino each of which is optionally substituted by C 1-3 alkyl; piperazino optionally substituted in the 4-position by acyl, carbethoxy, carbamoyl or C 1-3 alkyl; or a dialkanolamino or aminoalkylamino; and R 3 is hydrogen or methyl and said addition salts thereof may be prepared by (a) reacting a compound II wherein one or both of Z 1 and Z 2 are groups replaceable by amino and the other Z group if not replaceable by amino is R 1 or R 2 as above, with an amine R 1 -H or R 2 H; (b) removing or introducing an acyl or carbethoxy group from or into a piperazine ring; (c) oxidizing a thiomorpholine group to 1-oxido or 1,1-dioxido-thiomorpholine; (d) reacting a compound VI with crotonaldehyde, acrolein or glycerine in the presence of an oxidizing agent and an acidic condensation agent. The intermediates VI may be formed from 2,4-dichloro-5-nitro-pyrimidine by introducing the R 1 and R 2 by a process corresponding to (a) followed by reduction of the nitro group to amino. The intermediates II may be formed by converting (a) keto to chloro, (b) chloro to thiol, (c) thiol to alkylsulphonyl, or (d) chloro to phenoxy followed where applicable by introduction of one of the groups R 1 and R 2 . Pharmaceutical compositions of the compounds I inhibit aggregation of thrombocytes in human blood when administered orally, rectally or parenterally. Certain compounds I also have blood pressure lowering properties.
GB1621272A 1971-04-10 1972-04-07 Substituted pyrido-3,2-d-pyrimidines Expired GB1382487A (en)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
DE19712117657 DE2117657B2 (en) 1971-04-10 1971-04-10 PYRIDO SQUARE BRACKET ON 3.2-ANGLE BRACKET FOR PYRIMIDINE
DE19722202367 DE2202367A1 (en) 1972-01-19 1972-01-19 Pyrido(3,2-d)pyrimidines - anticoagulants
DE19722208534 DE2208534A1 (en) 1972-02-23 1972-02-23 Pyrido(3,2-d)pyrimidines - anticoagulants
DE19722208535 DE2208535A1 (en) 1972-02-23 1972-02-23 Pyrido(3,2-d)pyrimidines - anticoagulants

Publications (1)

Publication Number Publication Date
GB1382487A true GB1382487A (en) 1975-02-05

Family

ID=27431239

Family Applications (1)

Application Number Title Priority Date Filing Date
GB1621272A Expired GB1382487A (en) 1971-04-10 1972-04-07 Substituted pyrido-3,2-d-pyrimidines

Country Status (8)

Country Link
BE (1) BE781900A (en)
CA (1) CA992081A (en)
DD (1) DD97204A5 (en)
GB (1) GB1382487A (en)
HU (1) HU164346B (en)
IE (1) IE36269B1 (en)
IL (1) IL39174A (en)
NL (1) NL7204783A (en)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0404355A1 (en) * 1989-05-30 1990-12-27 Smithkline Beecham Intercredit B.V. Pyridopyrimidine derivatives, process for the preparation thereof and pharmaceutical compositions containing them

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0404355A1 (en) * 1989-05-30 1990-12-27 Smithkline Beecham Intercredit B.V. Pyridopyrimidine derivatives, process for the preparation thereof and pharmaceutical compositions containing them

Also Published As

Publication number Publication date
IE36269L (en) 1972-10-10
NL7204783A (en) 1972-10-12
IL39174A (en) 1975-02-10
BE781900A (en) 1972-10-10
IL39174A0 (en) 1972-06-28
IE36269B1 (en) 1976-09-29
CA992081A (en) 1976-06-29
DD97204A5 (en) 1973-04-20
HU164346B (en) 1974-01-28

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Legal Events

Date Code Title Description
PS Patent sealed [section 19, patents act 1949]
PLNP Patent lapsed through nonpayment of renewal fees