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Guanidinothiazole compounds, process for preparation and gastric inhibiting compositions containing them

Assignee: Astellas Pharma Inc
•
Filing: 1979-12-27
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Granted: 1981-08-11
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Expires: 1999-12-27
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Abstract

Abstract Novel guanidinothiazole compounds of the general formula <IMAGE> wherein R represents a hydrogen atom or a lower alkyl group, R1 represents an amino group, a lower alkyl group, a halogeno lower alkyl group, a substituted- or unsubstituted-aryl group, a mono- or di-lower alkylamino group, an arylamino group or an aralkylamino group, R2 represents a hydrogen atom, a lower alkyl group, a lower alkenyl group or a lower alkynyl group, Y represents a sulfur atom or a methylene group, m and n, each represents an integer of 1-3, and the pharmacologically acceptable acid addition salts thereof, they are useful as gastric acid secretion inhibitors.

Inventors

  • 👤 Yasufumi Hirata
  • 👤 Isao Yanagisawa
  • 👤 Yoshio Ishii
  • 👤 Shinichi Tsukamoto
  • 👤 Noriki Ito
  • 👤 Yasuo Isomura
  • 👤 Masaaki Takeda

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-04 02:45
CPC Classifications
C; C07; C07D; C07D277/00; C07D277/02; C07D277/20; C07D277/32; C07D277/38; C07D277/44; C07D277/48; A; A61; A61P; A61P1/00; A61P1/04; A61P43/00; C07D277/40

Claims Analysis

Total Claims: 8
Claim 1
Independent Claim 106 words
Guanidinothiazole compounds of the formula ##STR34## wherein R represents a hydrogen atom or a lower alkyl group, R 1 represents an amino group, a lower alkyl group, a halogeno lower alkyl group, a phenyl or naphthyl group which is unsubstituted or substituted by halogen, hydroxyl, amino, or alkoxy, a mono- or di-lower alkylamino group, an arylamino group or an aralkylamino group, R 2 represents a hydrogen atom, a lower alkyl group, a lower alkenyl group or a lower alkynyl group, Y represents a sulfur atom or a methylene group, m and n, each represents an integer of 1-3, and the pharmacologically acceptable acid addition salts thereof.
Claim 2
Dependent Claim 106 words
Guanidinothiazole compounds of the formula ##STR34## wherein R represents a hydrogen atom or a lower alkyl group, R 1 represents an amino group, a lower alkyl group, a halogeno lower alkyl group, a phenyl or naphthyl group which is unsubstituted or substituted by halogen, hydroxyl, amino, or alkoxy, a mono- or di-lower alkylamino group, an arylamino group or an aralkylamino group, R 2 represents a hydrogen atom, a lower alkyl group, a lower alkenyl group or a lower alkynyl group, Y represents a sulfur atom or a methylene group, m and n, each represents an integer of 1-3, and the pharmacologically acceptable acid addition salts thereof.
Claim 3
Dependent Claim 27 words
The compounds as claimed in claim 1 wherein R and R 2 are hydrogen atoms, R 1 is an amino group and Y is a sulfur atom.
Claim 4
Dependent Claim 19 words
The compounds as claimed in claim 1 wherein R 2 is a hydrogen atom or a lower alkyl group.
Claim 5
Dependent Claim 10 words
The compound as claimed in claim 1 which is N-sulfamoyl-3-[(2-guanidinothiazol-4-yl)methylthio]propionamidine.
Claim 6
Dependent Claim 10 words
The compound as claimed in claim 1 which is N-methansulfonyl-3-[(2-guanidinothiazol-4-yl)methylthio]propionamidine.
Claim 7
Dependent Claim 122 words
Medical composition containing a gastric acid secretion inhibiting amount of a guanidinothiazole compound of the formula ##STR35## wherein R represents a hydrogen atom or a lower alkyl group, R 1 represents an amino group, a lower alkyl group, a halogeno lower alkyl group, a phenyl or naphthyl group which is unsubstituted or substituted by halogen, hydroxyl, amino, or akoxy, a mono- or di-lower alkylamino group, an arylamino group or an aralkylamino group, R 2 represents a hydrogen atom, a lower alkyl group, a lower alkenyl group or a lower alkynyl group, Y represents a sulfur atom or a methylene group, m and n, each represent an integer of 1-3, or a non-toxic acid addition salt thereof and pharmaceutically acceptable carriers or diluents.
Claim 8
Dependent Claim 122 words
Medical composition containing a gastric acid secretion inhibiting amount of a guanidinothiazole compound of the formula ##STR35## wherein R represents a hydrogen atom or a lower alkyl group, R 1 represents an amino group, a lower alkyl group, a halogeno lower alkyl group, a phenyl or naphthyl group which is unsubstituted or substituted by halogen, hydroxyl, amino, or akoxy, a mono- or di-lower alkylamino group, an arylamino group or an aralkylamino group, R 2 represents a hydrogen atom, a lower alkyl group, a lower alkenyl group or a lower alkynyl group, Y represents a sulfur atom or a methylene group, m and n, each represent an integer of 1-3, or a non-toxic acid addition salt thereof and pharmaceutically acceptable carriers or diluents.

References Cited (Backward Citations)

US3950333A Cited
US4165378A Cited
US4165377A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1984-08-10 1985-02-09 1985-08-11 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1988-08-10 1989-02-09 1989-08-11 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1992-08-10 1993-02-09 1993-08-11 $7700.00 Window Closed / Lapsed

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