GB1021011A - Pyrazinoyl-guanidines - Google Patents

Pyrazinoyl-guanidines

Info

Publication number
GB1021011A
GB1021011A GB37991/62A GB3799162A GB1021011A GB 1021011 A GB1021011 A GB 1021011A GB 37991/62 A GB37991/62 A GB 37991/62A GB 3799162 A GB3799162 A GB 3799162A GB 1021011 A GB1021011 A GB 1021011A
Authority
GB
United Kingdom
Prior art keywords
amino
methyl
acid
aminopyrazinoyl
guanidines
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
GB37991/62A
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.)
Merck and Co Inc
Original Assignee
Merck and Co Inc
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
Application filed by Merck and Co Inc filed Critical Merck and Co Inc
Publication of GB1021011A publication Critical patent/GB1021011A/en
Expired legal-status Critical Current

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/53Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/63Compounds containing para-N-benzenesulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonyl hydrazide
    • A61K31/635Compounds containing para-N-benzenesulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonyl hydrazide having a heterocyclic ring, e.g. sulfadiazine

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material 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)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

The invention comprises (3-aminopyrazinoyl) guanidines having a halogen or trihalomethyl substituent attached to the pyrazine nucleus; salts thereof; and their preparation by reaction of C1- 5 alkyl esters of 3-aminopyrazinoic acid with guanidine prior or subsequent to halogenation. Pyrazine derivatives prepared as intermediates are: 2 - amino - or acetamido - 3 - methyl - 5 - fluoropyrazine, 3 - amino - 6 - fluoropyrazinoic acid and its methyl ester; 3-amino-5-hydroxypyrazinoic acid and its methyl ester, methyl 3-amino - 5 - chloro -or bromo - pyrazinoate; 3 - amino - 6 - (or 5 -) trifluoromethyl-pyrazinamide and the acid and methyl ester; methyl 3-chloroamino -or amino - 6 - chloropyrazinoate; methyl 3 - amino - 6 - bromopyrazinoate; (3-aminopyrazinoyl) guanidine; methyl 3-amino-6-iodopyrazinoate.ALSO:Pharmaceutical and veterinary compositions comprise (3-aminopyrazinoyl) guanidines having a halogen or trihalomethyl substitutent attached to the pyrazine nucleus, or their acid addition salts, in association with diluents or carriers. Electrolyte excretion patterns are modified, forms specified being for oral (tablets, pills, capsules) and parenteral administration. Other therapeutic agents embodiable are diuretics hypotensives and steroids (e.g. thiazides, acetazolamide, benzothiadiazines, chlormerodrin, dichlorphenamide, chlorthalidone, chlorazanil, 4-(2-methylenebutyryl)-2, 3-dichlorphenoxy-acetic acid).
GB37991/62A 1961-10-12 1962-10-08 Pyrazinoyl-guanidines Expired GB1021011A (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US14455661A 1961-10-12 1961-10-12

Publications (1)

Publication Number Publication Date
GB1021011A true GB1021011A (en) 1966-02-23

Family

ID=22509116

Family Applications (1)

Application Number Title Priority Date Filing Date
GB37991/62A Expired GB1021011A (en) 1961-10-12 1962-10-08 Pyrazinoyl-guanidines

Country Status (7)

Country Link
CH (2) CH446344A (en)
CY (1) CY373A (en)
DE (1) DE1470030B1 (en)
DK (1) DK117147B (en)
ES (1) ES281789A1 (en)
FR (1) FR2259M (en)
GB (1) GB1021011A (en)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3191631A (en) * 1963-05-06 1965-06-29 Callahan Mining Corp Flexible hose

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BE596467A (en) * 1960-10-27 1961-04-27 Smith Kline French Lab New medicinal compositions with strong diuretic and hypotensive activities.

Also Published As

Publication number Publication date
CH446344A (en) 1967-11-15
CH446351A (en) 1967-11-15
ES281789A1 (en) 1963-02-01
FR2259M (en) 1964-01-06
DE1470030B1 (en) 1970-03-12
DK117147B (en) 1970-03-23
CY373A (en) 1967-02-24

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