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Adamantane derivatives in the prevention and treatment of cerebral ischemia
Authors: Joachim Bormann, Markus R. Gold, Wolfgang Schatton
Patent US 5061703 (1991) C. A. 1992 №.........
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Последний раз редактировалось Legalny Пт авг 14, 2015 2:28 pm, всего редактировалось 1 раз.
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есть в Family list: US5061703 (A) ― 1991-10-29 ссылка на EP 392059 A1, который упоминается в SF
Use of adamantane derivatives in the prevention and treatment of cerebral ischemia. Bormann, Joachim; Gold, Markus R.; Schatton, Wolfgang. (Merz und Co. G.m.b.H. und Co., Germany). Eur. Pat. Appl. (1990), 16 pp. CODEN:EPXXDW EP 392059 A1 19901017 Designated States R: AT, BE, CH, DE, ES, FR, GB, GR, IT, LI, LU, NL, SE. Patent written in German. Application: EP 1989-106657 19890414. Priority: EP 1989-106657 19890414. CAN 115:22231 AN 1991:422231 CAPLUS
Adamantane derivs. I (R1, R2, R5 = H, C1-6 alkyl, or R1NR2 = cyclic C4N or C5N; R3, R4 = H, C1-6 alkyl, C5-6 cycloalkyl, Ph) and their salts are useful for prevention and treatment of cerebral ischemia and Alzheimer's disease. Thus, I (R1 = R2 = R5 = H; R3 = R4 = Me) (II), administered to rats (20 mg/kg i.p.) 1 h before application of carotid clamping and hypotension (60-80 mmHg, by blood withdrawal) for 10 min, diminished the no. of damaged neurons in the CA1 region of the hippocampus from 80.2 to 53.1%. II also showed anticonvulsant and N-methyl-D-aspartic acid receptor-blocking activity. Tablets were prepd. contg. I 10.0, lactose 67.5, microcryst. cellulose 18.0, and talc 4.5 mg. I-HCl (R1 = R2 = R4 = R5 = H, R3 = cyclohexyl) was prepd. by converting 1-bromoadamantane to 1-phenyladamantane with FeCl3 in C6H6, then to 1-hydroxy-3-phenyladmantane with CrO3, in 3 further steps to 1-amino-3-phenyladamantane-HCl, and hydrogenating over PtO2/C
Use of adamantane derivatives in the prevention and treatment of cerebral ischemia. Bormann, Joachim; Gold, Markus R.; Schatton, Wolfgang. (Merz und Co. G.m.b.H. und Co., Germany). Eur. Pat. Appl. (1990), 16 pp. CODEN:EPXXDW EP 392059 A1 19901017 Designated States R: AT, BE, CH, DE, ES, FR, GB, GR, IT, LI, LU, NL, SE. Patent written in German. Application: EP 1989-106657 19890414. Priority: EP 1989-106657 19890414. CAN 115:22231 AN 1991:422231 CAPLUS
Adamantane derivs. I (R1, R2, R5 = H, C1-6 alkyl, or R1NR2 = cyclic C4N or C5N; R3, R4 = H, C1-6 alkyl, C5-6 cycloalkyl, Ph) and their salts are useful for prevention and treatment of cerebral ischemia and Alzheimer's disease. Thus, I (R1 = R2 = R5 = H; R3 = R4 = Me) (II), administered to rats (20 mg/kg i.p.) 1 h before application of carotid clamping and hypotension (60-80 mmHg, by blood withdrawal) for 10 min, diminished the no. of damaged neurons in the CA1 region of the hippocampus from 80.2 to 53.1%. II also showed anticonvulsant and N-methyl-D-aspartic acid receptor-blocking activity. Tablets were prepd. contg. I 10.0, lactose 67.5, microcryst. cellulose 18.0, and talc 4.5 mg. I-HCl (R1 = R2 = R4 = R5 = H, R3 = cyclohexyl) was prepd. by converting 1-bromoadamantane to 1-phenyladamantane with FeCl3 in C6H6, then to 1-hydroxy-3-phenyladmantane with CrO3, in 3 further steps to 1-amino-3-phenyladamantane-HCl, and hydrogenating over PtO2/C
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