IT1206451B - Piperazino-alkyl di:hydro-pyridine 3-carboxylate ester - Google Patents
Piperazino-alkyl di:hydro-pyridine 3-carboxylate esterInfo
- Publication number
- IT1206451B IT1206451B IT8321043A IT2104383A IT1206451B IT 1206451 B IT1206451 B IT 1206451B IT 8321043 A IT8321043 A IT 8321043A IT 2104383 A IT2104383 A IT 2104383A IT 1206451 B IT1206451 B IT 1206451B
- Authority
- IT
- Italy
- Prior art keywords
- alkyl
- substd
- opt
- cooy
- alkoxy
- Prior art date
Links
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 title 1
- 150000002148 esters Chemical class 0.000 title 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 3
- 125000000217 alkyl group Chemical group 0.000 abstract 3
- 125000002252 acyl group Chemical group 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 abstract 1
- 206010002383 Angina Pectoris Diseases 0.000 abstract 1
- 208000024172 Cardiovascular disease Diseases 0.000 abstract 1
- 206010020772 Hypertension Diseases 0.000 abstract 1
- 241000699670 Mus sp. Species 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 1
- 125000002947 alkylene group Chemical group 0.000 abstract 1
- 125000001246 bromo group Chemical group Br* 0.000 abstract 1
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 1
- 125000001951 carbamoylamino group Chemical group C(N)(=O)N* 0.000 abstract 1
- 125000001309 chloro group Chemical group Cl* 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 125000004925 dihydropyridyl group Chemical class N1(CC=CC=C1)* 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 125000001153 fluoro group Chemical group F* 0.000 abstract 1
- -1 hydroxy, amino Chemical group 0.000 abstract 1
- 239000000543 intermediate Substances 0.000 abstract 1
- 238000001990 intravenous administration Methods 0.000 abstract 1
- 208000028867 ischemia Diseases 0.000 abstract 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 1
- 125000006501 nitrophenyl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000003396 thiol group Chemical class [H]S* 0.000 abstract 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 1
Abstract
Dihydropyridine esters of formula (I), their racemates, enantiomers diastereoisomers and pharmaceutically acceptable acid addn. salts are new. In (I) Y is (II), R1 is 1-5C alkyl, opt. substd. by alkoxy. R2 is phenyl or nitrophenyl. R3 is phenyl (opt. substd. by 1-3 of 1-4C alkyl or alkoxy, fluoro, chloro, bromo, nitro, cyano, 2-5C alkoxycarbonyl, trifluoromethyl, hydroxy, amino (opt. substd. by 1 or 2 alkyl or acyl), mercapto, alkyl S(O)n (n is 0-2), 1-5C acyl, carbamoyl or ureido) or is 5-6 membered monocyclic heteroaryl contg. 1 or more N, O or S. X is linear or branched 2-5C alkylene, opt. substd. by alkoxy. Also new are the intermediates (II), (III) and (IV): CH3.CO.CH2.COOY (II) CH3.C(NH2)=CH.COOY (III) CH3.CO.C(COOY)=CHR2 (IV). (I) have calcium-antagonising activity so are useful for treating and preventing hypertension, angina, ischaemia and other cardiovascular disorders. The daily dose is 5-50 mg, 1-3 times daily, and in mice most cpds. had intravenous LD50 over 15 mg per kg.
Priority Applications (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IT8321043A IT1206451B (en) | 1983-05-11 | 1983-05-11 | Piperazino-alkyl di:hydro-pyridine 3-carboxylate ester |
| AT83105196T ATE35677T1 (en) | 1982-06-03 | 1983-05-26 | DIHYDROPYRIDINS WITH CALCIUM ANTAGONIST ACTIVITIES, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM. |
| DE8383105196T DE3377352D1 (en) | 1982-06-03 | 1983-05-26 | Dihydropyridines with an antagonistic activity to calcium, process for their preparation, and pharmaceutical compositions containing them |
| EP83105196A EP0097821B1 (en) | 1982-06-03 | 1983-05-26 | Dihydropyridines with an antagonistic activity to calcium, process for their preparation, and pharmaceutical compositions containing them |
| ES522883A ES8503213A1 (en) | 1982-06-03 | 1983-06-01 | Dihydropyridines with an antagonistic activity to calcium, process for their preparation, and pharmaceutical compositions containing them. |
| AU15284/83A AU541067B2 (en) | 1982-06-03 | 1983-06-01 | 2,6-dimethyl-3,5-dicarboxylates-1,4-dihydropyridines |
| US06/563,008 US4894460A (en) | 1982-06-03 | 1983-12-19 | Basic esters exhibiting an antagonistic activity to calcium, process for the preparation thereof and pharmaceutical compositions therefrom |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IT8321043A IT1206451B (en) | 1983-05-11 | 1983-05-11 | Piperazino-alkyl di:hydro-pyridine 3-carboxylate ester |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| IT8321043A0 IT8321043A0 (en) | 1983-05-11 |
| IT1206451B true IT1206451B (en) | 1989-04-27 |
Family
ID=11175853
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IT8321043A IT1206451B (en) | 1982-06-03 | 1983-05-11 | Piperazino-alkyl di:hydro-pyridine 3-carboxylate ester |
Country Status (1)
| Country | Link |
|---|---|
| IT (1) | IT1206451B (en) |
-
1983
- 1983-05-11 IT IT8321043A patent/IT1206451B/en active
Also Published As
| Publication number | Publication date |
|---|---|
| IT8321043A0 (en) | 1983-05-11 |
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