IT1156749B - Amino-alkyl substd. thiophene derivs. - selective blockers of histamine H2 receptors, e.g. for treating gastric hypersecretion - Google Patents
Amino-alkyl substd. thiophene derivs. - selective blockers of histamine H2 receptors, e.g. for treating gastric hypersecretionInfo
- Publication number
- IT1156749B IT1156749B IT4940378A IT4940378A IT1156749B IT 1156749 B IT1156749 B IT 1156749B IT 4940378 A IT4940378 A IT 4940378A IT 4940378 A IT4940378 A IT 4940378A IT 1156749 B IT1156749 B IT 1156749B
- Authority
- IT
- Italy
- Prior art keywords
- histamine
- receptors
- formula
- opt
- lower alkyl
- Prior art date
Links
- YTPLMLYBLZKORZ-UHFFFAOYSA-N Thiophene Chemical compound C=1C=CSC=1 YTPLMLYBLZKORZ-UHFFFAOYSA-N 0.000 title abstract 4
- 102000003710 Histamine H2 Receptors Human genes 0.000 title abstract 2
- 108090000050 Histamine H2 Receptors Proteins 0.000 title abstract 2
- 229930192474 thiophene Natural products 0.000 title abstract 2
- 125000004103 aminoalkyl group Chemical group 0.000 title 1
- 230000002496 gastric effect Effects 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 4
- NTYJJOPFIAHURM-UHFFFAOYSA-N Histamine Chemical compound NCCC1=CN=CN1 NTYJJOPFIAHURM-UHFFFAOYSA-N 0.000 abstract 2
- 125000003342 alkenyl group Chemical group 0.000 abstract 2
- 125000004390 alkyl sulfonyl group Chemical group 0.000 abstract 2
- 125000004391 aryl sulfonyl group Chemical group 0.000 abstract 2
- 208000010668 atopic eczema Diseases 0.000 abstract 2
- 101100244083 Arabidopsis thaliana PKL gene Proteins 0.000 abstract 1
- 208000024780 Urticaria Diseases 0.000 abstract 1
- 125000004450 alkenylene group Chemical group 0.000 abstract 1
- 125000004183 alkoxy alkyl group Chemical group 0.000 abstract 1
- 230000000172 allergic effect Effects 0.000 abstract 1
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 210000004211 gastric acid Anatomy 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 229960001340 histamine Drugs 0.000 abstract 1
- 150000004677 hydrates Chemical class 0.000 abstract 1
- 238000001727 in vivo Methods 0.000 abstract 1
- 239000000543 intermediate Substances 0.000 abstract 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 1
- 239000002243 precursor Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Thiophene derivs. of formula (I), their physiologically acceptable salts, hydrates and in vivo precursors are new: In the formula, R1 and R2 = H, lower alkyl, cycloalkyl, aralkyl or alkenyl, the alkyl groups opt. interrupted by O or NR4; or R1R2N is a heterocycle opt. contg. other O or NR4 functions; R4 = H, lower alkyl, alkenyl or alkoxyalkyl; X is O,S or CH2; Y is S,O=NR5 or =CHR6; R5 = H, NO2, CN, lower alkyl, aryl, alkylsulphonyl or arylsulphonyl; R6 = NO2, alkylsulphonyl or arylsulphonyl; m=2-4, n = 1 or 2; or can also be O when X is S or CH2; and alk = 1-6C opt. branched alkenylene (sic). Also new are intermediates of formula (II). (I) selectively block the histamine H2 receptors so are useful in treatment of hypersecretion of gastric acid; allergic states in which histamine is a mediator, and allergic-inflammatory conditions such as urticaria. The usual oral dose is 0.1-2g/day; they can also be given topically or parenterally.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
GB20659/77A GB1601459A (en) | 1977-05-17 | 1977-05-17 | Aminoalkyl thiophene derivatives |
IE853/78A IE46811B1 (en) | 1977-05-17 | 1978-04-28 | Aminoalkyl thiophene derivatives |
Publications (2)
Publication Number | Publication Date |
---|---|
IT7849403A0 IT7849403A0 (en) | 1978-05-16 |
IT1156749B true IT1156749B (en) | 1987-02-04 |
Family
ID=26254808
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
IT4940378A IT1156749B (en) | 1977-05-17 | 1978-05-16 | Amino-alkyl substd. thiophene derivs. - selective blockers of histamine H2 receptors, e.g. for treating gastric hypersecretion |
Country Status (1)
Country | Link |
---|---|
IT (1) | IT1156749B (en) |
-
1978
- 1978-05-16 IT IT4940378A patent/IT1156749B/en active
Also Published As
Publication number | Publication date |
---|---|
IT7849403A0 (en) | 1978-05-16 |
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