GB1145934A - Access for the preparation of pyrazinoyl- and pyrazinamido-guanidines - Google Patents

Access for the preparation of pyrazinoyl- and pyrazinamido-guanidines

Info

Publication number
GB1145934A
GB1145934A GB2621767A GB2621767A GB1145934A GB 1145934 A GB1145934 A GB 1145934A GB 2621767 A GB2621767 A GB 2621767A GB 2621767 A GB2621767 A GB 2621767A GB 1145934 A GB1145934 A GB 1145934A
Authority
GB
United Kingdom
Prior art keywords
alkyl
phenyl
pyrazinamido
pyrazinoyl
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
GB2621767A
Inventor
Peter Immanuel Pollak
Roger James Tull
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 GB1145934A publication Critical patent/GB1145934A/en
Expired legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D241/24—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D241/26—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms directly attached to ring carbon atoms

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

1,145,934. (3,5-Diamino-6-chloro-pyrazinoyl and -pyrazinamido)-guanidines. MERCK & CO. Inc. 7 June, 1967 [25 Aug., 1966], No. 26217/67. Heading C2C. (3,5 - Diamino - 6 - chloro - pyrazinoyl and -pyrazinamido)-guanidines of the general formula wherein R<SP>1</SP> and R<SP>2</SP>, which are the same or different, are hydrogen, C 1-5 alkyl or phenyl-C 1-5 alkyl; R<SP>3</SP> is hydrogen, C 1-5 alkyl, hydroxy- C 1-5 alkyl, pyridyl-C 1-5 alkyl, phenyl-C 1-5 alkyl, halophenyl-C 1-5 alkyl, (C 1-5 alkyl-phenyl)-C 1-5 alkyl or (C 1-5 alkoxy-phenyl)-C 1-5 alkyl; R<SP>4</SP> is hydrogen, C 1-5 alkyl, phenyl-C 1-5, alkyl, halophenyl-C 1-5 alkyl, (C 1-5 alkylphenyl)-C 1-5 alkyl or (C 1-5 alkoxy-phenyl)-C 1-5 alkyl; or R<SP>3</SP> and R<SP>4</SP> are linked together to form, with the nitrogen atom to which they are attached, a group having the formula wherein x is 4, 5, 6 or 7; R<SP>5</SP> is hydrogen or C 1-5 alkyl; or R<SP>4</SP> and R<SP>5</SP> are linked together to form an ethylene or trimethylene radical; and n is 0 or 1; and acid addition salts thereof are prepared by reaction of a (3,5-diamino-pyrazinoyl or -pyrazinamido)-guanidine of the general formula with chlorine, followed by optional conversion of the product to an acid addition salt thereof. (3,5 - Diamino - pyrazinoyl or - pyrazinamido)-guanidines of the second general formula above are prepared by reaction of a C 1-5 alkyl ester of a 3-amino-5-NR<SP>1</SP>R<SP>2</SP>-pyrazinoate with a guanidine or aminoguanidine of the general formula
GB2621767A 1966-08-25 1967-06-07 Access for the preparation of pyrazinoyl- and pyrazinamido-guanidines Expired GB1145934A (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US57492266A 1966-08-25 1966-08-25

Publications (1)

Publication Number Publication Date
GB1145934A true GB1145934A (en) 1969-03-19

Family

ID=24298194

Family Applications (1)

Application Number Title Priority Date Filing Date
GB2621767A Expired GB1145934A (en) 1966-08-25 1967-06-07 Access for the preparation of pyrazinoyl- and pyrazinamido-guanidines

Country Status (8)

Country Link
BE (1) BE699438A (en)
CH (1) CH487169A (en)
DE (1) DE1695421A1 (en)
ES (1) ES341324A1 (en)
GB (1) GB1145934A (en)
IL (1) IL27897A (en)
NL (1) NL6707570A (en)
SE (1) SE333146B (en)

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2011506386A (en) * 2007-12-10 2011-03-03 ノバルティス アーゲー Organic compounds
US9586911B2 (en) 2013-12-13 2017-03-07 Parion Sciences, Inc. Arylalkyl- and aryloxyalkyl-substituted epthelial sodium channel blocking compounds
US9695134B2 (en) 2012-12-17 2017-07-04 Parion Sciences, Inc. 3,5-diamino-6-chloro-N-(n-(4-phenylbutyl)carbamimidoyl)pyrazine-2-carboxamide compounds
US10071970B2 (en) 2012-12-17 2018-09-11 Parion Sciences, Inc. Chloro-pyrazine carboxamide derivatives with epithelial sodium channel blocking activity
US10167266B2 (en) 2002-02-19 2019-01-01 Parion Sciences, Inc. Sodium channel blockers
US10752597B2 (en) 2011-06-27 2020-08-25 Parion Sciences, Inc. 3,5-diamino-6-chloro-N—(N-(4-(4-(2-(hexyl(2,3,4,5,6-pentahydroxyhexyl)amino)ethoxy)phenyl)butyl)carbamimidoyl)pyrazine-2-carboxamide

Cited By (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10167266B2 (en) 2002-02-19 2019-01-01 Parion Sciences, Inc. Sodium channel blockers
JP2011506386A (en) * 2007-12-10 2011-03-03 ノバルティス アーゲー Organic compounds
US8697687B2 (en) 2007-12-10 2014-04-15 Novartis Ag Treating diseases mediated by blockade of the epithelial sodium channel with pyrazine-2-carboxamide derivatives
US9139586B2 (en) 2007-12-10 2015-09-22 Novartis Ag Treating diseases mediated by blockade of the epithelial sodium channel with pyrazine-2-carboxamide derivatives
US9643983B2 (en) 2007-12-10 2017-05-09 Novartis Ag Treating diseases mediated by blockade of the epithelial sodium channel with pyrazine-2-carboxamide derivatives
US10752597B2 (en) 2011-06-27 2020-08-25 Parion Sciences, Inc. 3,5-diamino-6-chloro-N—(N-(4-(4-(2-(hexyl(2,3,4,5,6-pentahydroxyhexyl)amino)ethoxy)phenyl)butyl)carbamimidoyl)pyrazine-2-carboxamide
US11578042B2 (en) 2011-06-27 2023-02-14 Parion Sciences, Inc. 3,5-diamino-6-chloro-N-(N-(4-(4-(2-(hexyl(2,3,4,5,6-pentahydroxyhexyl)amino)ethoxy)phenyl)butyl)carbamimidoyl)pyrazine-2-carboxamide
US9695134B2 (en) 2012-12-17 2017-07-04 Parion Sciences, Inc. 3,5-diamino-6-chloro-N-(n-(4-phenylbutyl)carbamimidoyl)pyrazine-2-carboxamide compounds
US10071970B2 (en) 2012-12-17 2018-09-11 Parion Sciences, Inc. Chloro-pyrazine carboxamide derivatives with epithelial sodium channel blocking activity
US9586911B2 (en) 2013-12-13 2017-03-07 Parion Sciences, Inc. Arylalkyl- and aryloxyalkyl-substituted epthelial sodium channel blocking compounds
US9957238B2 (en) 2013-12-13 2018-05-01 Parion Sciences, Inc. Arylalkyl-and aryloxyalkyl-substituted epithelial sodium channel blocking compounds
US10233158B2 (en) 2013-12-13 2019-03-19 Parion Sciences, Inc. Arylalkyl- and aryloxyalkyl-substituted epithelial sodium channel blocking compounds

Also Published As

Publication number Publication date
ES341324A1 (en) 1968-10-01
IL27897A (en) 1972-02-29
SE333146B (en) 1971-03-08
DE1695421A1 (en) 1971-04-15
BE699438A (en) 1967-12-04
CH487169A (en) 1970-03-15
NL6707570A (en) 1968-02-26

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