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Application

99124224/04, 1999-11-15

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Start date

1999-11-15

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Actual filing date

1999-11-15

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Published

2001-10-10

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Inventor

Dolgo-Saburov V.B.Kosmachev A.B.Evdokimova E.A.Libman N.M.Ramsh S.M.Petrov V.V.Tonkopij V.D.Fil'Ko O.A.Kubarskaja L.G.

(73)

Holder

Gosudarstvennoe Uchrezhdenie Nauki Institut Toksikologii

HYDROCHLORIDES OF SUBSTITUTED ACETYLENIC AMINOALCOHOL-ACTIVE AND LOW-TOXIC HALOPERIDOL ANTAGONISTS Russian patent published in 2001 - IPC

Abstract RU 2174510 C2

FIELD: medicine. SUBSTANCE: described are new substituted acetylenic aminoalcohol hydrochlorides of general formula 1 R¹R²C(OH)CH₂C≡CCH₂Am•HCl which have low toxicity and have properties of haloperidol antagonists which are useful in medicine for treatment and prophylaxis of parkinsonism. In general formula 1 R¹,R² and Am are as defined in 1a: C₆H₅, cyclopentyl, N[CH(CH₃)₂]₂; 1b: C₆H₅, cyclopentyl, pyrrolidino; 1c: C₆H₅, cyclopentyl, piperidono; 1d: cyclopentyl, C₆H₅,N(CH₂CH₃)₂; 1e: cyclopentyl, C₆H₅, pyrrolidino; 1f: R¹ and R² together form group A; Am is ; 1g: N(CH₂CH₃)₂ and R¹ and R² together form said group A, and Am is pyrrolidino. Compounds are prepared using Mannich reaction by reacting corresponding amino compound and acetylenic alcohol in the presence of copper salts. EFFECT: improved properties of compounds. 2 tbl

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RU 2 174 510 C2

Authors

Dolgo-Saburov V.B.

Kosmachev A.B.

Evdokimova E.A.

Libman N.M.

Ramsh S.M.

Petrov V.V.

Tonkopij V.D.

Fil'Ko O.A.

Kubarskaja L.G.

Dates

2001-10-10—Published

1999-11-15—Filed