发明名称 |
2-CYCLIC AMINO-2-(1,2-BENZISOXAZOL-3-YL)ACETIC ACID ESTER DERIVATIVES, PROCESS FOR THE PREPARATION THEREOF AND COMPOSITION CONTAINING THE SAME |
摘要 |
<p>2-Cyclic amino-2-[1,2-benzisoxazol-3-yl]acetic acid derivatives of the formula: …<CHEM>… (wherein R1 is hydrogen or a halogen atom, R2 is a lower alkyl group, Am is a 5- to 9-membered saturated cyclic amino group which may be substituted by a lower alkyl group, and the piperidine moiety is attached at its 3- or 4-position), and their pharmaceutically acceptable acid addition salts and quaternary ammonium salts have potent anticholinergic antispasmodic activity, while they are weak in side effects such as mydriasis, inhibition of salivary secretion and tachycardia. The preferred compounds are …<CHEM>… and the 1-ethyl-1-methyl piperidinium iodide derivative thereof. …<??>Compounds (I) may be made from Am-H and a 2-haloacetic acid derivative (whose synthesis is described). They can be selectively quaternised at the piperidine N-atom.</p> |
申请公布号 |
EP0073645(A3) |
申请公布日期 |
1984.03.28 |
申请号 |
EP19820304477 |
申请日期 |
1982.08.25 |
申请人 |
DAINIPPON PHARMACEUTICAL CO., LTD. |
发明人 |
NISHIMURA, HARUKI;NARUTO, SHUNSUKE;MIZUTA, HIROYUKI;KODAKAWA, TOSHIAKI;KAWASHIMA, KATSUYOSHI |
分类号 |
B60G11/26;C07D261/20;A61K31/42;A61K31/423;B60G11/56;B60G17/015;B62D53/06;B62D53/08;C07D413/06;C07D413/12;C07D413/14;(IPC1-7):07D413/12;07D413/14;61K31/445;61K31/42 |
主分类号 |
B60G11/26 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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