Title:
MITIGATION OF BETA-ADRENERGIC BLOCKING AGENT
Document Type and Number:
Japanese Patent JP2561034
Kind Code:
B2
Abstract:
PURPOSE: To mitigate a β-adrenergic blocking agent so as to be transformed into an inert metabolite in one step simply and in a predictable and controllable way.
CONSTITUTION: A β-adrenergic blocking agent having a structural portion of formula I is mitigated so as to be transformed into a compound of formula II {(n) is 0-10; R is a 6-12C cycloalkyl-CpH2p ((p) is 0-3), 6-12C cycloalkenyl-CpH2p, CH2-X-R3 (X is S, SO2 or SO; R2 is a 1-7C alkyl or 3-12C cycloalkyl), CH2- S+(CH3)-R2 or CH(R3)-X-R4 [R3 and R4 are each a 1-7C alkyl or joined together into (CH2)m ((m) is 3 or 4)], etc.; R1 is a 1-7C alkyl; Ar is a divalent group containing at least one aromatic nucleus}. The compound of formula II is obtained by reaction of a compound of formula III (Z is a group of formula IV or formula V) with an amine of the formula MH2R1, and has excellent blocking effect without any side effect over a certain duration depending on hydrolytic metabolic rate alone.
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Inventors:
BOODAA NIKORASU ESU
Application Number:
JP16159694A
Publication Date:
December 04, 1996
Filing Date:
July 13, 1994
Export Citation:
Assignee:
BODOR NICHOLAS S
International Classes:
C07C217/32; A61K31/215; A61K31/235; A61K31/34; A61K31/343; A61K31/40; A61K31/403; A61K31/404; A61K31/47; A61K31/535; A61P9/00; A61P9/10; A61P25/02; A61P27/02; A61P27/06; C07C67/00; C07C213/00; C07C217/18; C07C217/36; C07C231/00; C07C233/47; C07C233/52; C07C233/65; C07C235/06; C07C235/14; C07C235/16; C07C313/00; C07C317/18; C07C317/22; C07C317/44; C07C323/12; C07C323/52; C07C323/62; C07C381/12; C07D209/08; C07D215/22; C07D307/83; (IPC1-7): A61K31/215; A61K31/235; A61K31/34; A61K31/40; A61K31/47; A61K31/535; C07C217/32; C07D209/08; C07D215/22; C07D307/83
Domestic Patent References:
| JP57502123A |
Attorney, Agent or Firm:
Hirose Shoichi