KR970069997A - 2,3-benzodiazepine derivative - Google Patents

Abstract

Non-competitive AMPA antagonist compounds of formula (I), isomers thereof and acid addition salts of such compounds or isomers are disclosed. In addition, pharmaceutical compositions comprising any of the compounds, isomers and acid addition salts are disclosed. In the general formula, R ¹ and R ² are each independently hydrogen, halogen, C _1-4 alkyl group, C _1-4 alkoxy group, nitro group, trifluoromethyl group or group having the general formula of -NR ⁸ R ⁹ , R ⁸ and R ⁹ are each independently hydrogen, a C _1-4 alkyl group or a group having the general formula of —COR ¹⁰ , R ¹⁰ is hydrogen, a C _1-6 alkyl group which may be substituted, C _6-10 aryl Group, C _1-4 alkoxy group, C _3-5 cycloalkyl group, C _2-6 alkenyl group, C _3-5 cycloalkoxy group or a group having the general formula of —NR ¹¹ R ¹² , wherein R ¹¹ and R ¹² Each independently represent hydrogen, a C _1-4 alkyl group, a C _3-5 cycloalkyl group, or a C _6-10 aryl group, and R ³ represents a C _1-4 alkyl group, a C _3-5 cycloalkyl group, or a —CO—R ¹³ group. A group having the general formula wherein R ¹³ is the same as defined in relation to R ^10, and R ⁴ and R ⁵ each independently represent hydrogen or a C _1-3 alkyl group, and R ⁶ and R ⁷ Are each independently hydrogen, chlorine or bromine, but if one of R ⁶ and R ⁷ is hydrogen, the other must not be hydrogen.

The present invention also discloses starting materials of formula (II), wherein R ¹ , R ² , R ⁴ , R ⁵ , R ⁶ and R ⁷ have the same meanings as defined with respect to formula (I).

Description

2,3-benzodiazepine derivative

As this is a public information case, the full text was not included.

Claims (10)

A compound having the following general formula, an isomer of the compound, and an acid addition salt of the compound or the isomer. (In the general formula, R ¹ and R ² are each independently hydrogen, halogen, C _1-4 alkyl group, C _1-4 alkoxy group, nitro group, trifluoromethyl group or group having a general formula of -NR ⁸ R ⁹ R ⁸ and R ⁹ each independently represent a hydrogen, a C _1-4 alkyl group or a group having a general formula of —COR ¹⁰ , and R ¹⁰ is hydrogen, a C _1-6 alkyl group which may be substituted, C _6-10 An aryl group, a C _1-4 alkoxy group, a C _3-5 cycloalkyl group, a C _2-6 alkenyl group, a C _3-5 cycloalkoxy group or a group having the general formula of —NR ¹¹ R ¹² , wherein R ¹¹ and R ¹² each independently represents hydrogen, a C _1-4 alkyl group, a C _3-5 cycloalkyl group, or a C _6-10 aryl group, and R ³ represents a C _1-4 alkyl group, a C _3-5 cycloalkyl group, or -CO-R ¹³ Means a group having the general formula of wherein R ¹³ is as defined in relation to R ¹⁰ , R ⁴ and R ⁵ are each independently hydrogen or a C _1-3 alkyl group, R ⁶ and Each R ⁷ independently represents hydrogen, chlorine or bromine, but if one of R ⁶ and R ⁷ is hydrogen, the other must not be hydrogen) 3-acetyl-1- (4-aminophenyl) -8-chloro-4-methyl-4,5-dihydro-3H-2,3-benzodiazepine. 1- (4-aminophenyl) -8-chloro-4-methyl-3-methylcarbamoyl-4,5-dihydro-3H-2,3-benzodiazepine. R ¹ and R ⁷ are compounds of formula (I) as defined in claim 1, isomers thereof, or pharmaceutically acceptable acid addition salts of said compounds or said isomers for use in the preparation of pharmaceutical compositions, Pharmaceutical compositions containing as active ingredients using solvents, diluents and excipients. A drug using the compound of claim 1. A pharmaceutical composition useful for the treatment of diseases associated with muscle spasms, prepared using the compound of claim 1. A pharmaceutical composition useful for the treatment of epilepsy prepared using the compound of claim 1. A pharmaceutical composition useful for the treatment of acute or chronic neurodegenerative diseases, prepared using the compound of claim 1. R ¹ , R ² , R ³ , R ⁴ , R ⁵ , R ⁶ and R ⁷ have the same meanings as defined in claim 1, wherein R ¹ , R ² , R ⁴ , R ⁵ , R ⁶ and R ⁷ are Introducing a R ³ group at position 3 of the compound of formula (II) having the same meaning as described above, converting the compound of formula (I) to another compound of formula (I), and A process for preparing a compound of formula (I), isomers thereof and acid addition salts thereof, comprising converting the compound to an acid addition salt thereof or separating the compound of formula (I) from the acid addition salt. Compounds having the following general formula. (In the general formula, R ¹ and R ² are each independently hydrogen, halogen, C _1-4 alkyl group, C _1-4 alkoxy group, nitro group, trifluoromethyl group or group having a general formula of -NR ⁸ R ⁹ R ⁸ and R ⁹ each independently represent a hydrogen, a C _1-4 alkyl group or a group having a general formula of —COR ¹⁰ , and R ¹⁰ is hydrogen, a C _1-6 alkyl group which may be substituted, C _6-10 An aryl group, a C _1-4 alkoxy group, a C _3-5 cycloalkyl group, a C _2-6 alkenyl group, a C _3-5 cycloalkoxy group or a group having the general formula of —NR ¹¹ R ¹² , wherein R ¹¹ and R ¹² each independently represents hydrogen, a C _1-4 alkyl group, a C _3-5 cycloalkyl group, or a C _6-10 aryl group, R ³ represents hydrogen, and R ⁴ and R ⁵ each independently represents hydrogen or C _{1- 3} means an alkyl group, and R ⁶ and R ⁷ each independently represent hydrogen, chlorine or bromine, and if one of R ⁶ and R ⁷ is hydrogen, the other is not hydrogen do) ※ Note: The disclosure is based on the initial application.