Indole derivatives
AssigneeOtsuka Pharmaceutical Factory, Inc.
InventorsMasatoshi Inai, Tadanao Shibutani, Jun Kanaya, Masako Moritake, Akie Tanaka
Life of this patent
Estimating the term…
Abstract
The present invention provides indole derivatives of the general formula: ##STR1## The indole derivatives of the invention have potent antiestrogen activity and are useful as drugs for the treatment of estrogen-dependent diseases, such as anovulatory infertility, prostatic hypertrophy, osteoporosis, breast cancer, endometrial cancer and melanoma.
Claims8
An indole derivative of the general formula ##STR414## wherein R.sup.1 is a halogen atom, R.sup.2 is a hydrogen atom, a lower alkyl group, a lower alkanoyl group or a benzoyl group, R.sup.3 is a hydrogen atom, a lower alkyl group or a halogen atom, R.sup.4 is a group of the formula ##STR415## in which R.sup.6 is a lower alkyl group, a cycloalkyl group, a phenyl group which may optionally have a lower alkyl group as a substituent, a phenyl-lower alkyl group or a pyridyl group, R.sup.7 is a hydrogen atom or a lower alkyl group, Q is a sulfur or selenium atom and n is an integer of 0 to 2, A is an alkylene group, m is an integer of 0 to 1, R.sup.5 is a hydrogen atom, an alkyl group or a benzoyl group having a hydroxyl group or a group of the formula --O--B--R.sup.8 in which B is a lower alkylene group and R.sup.8 is a phenyl, di-lower alkyl-amino, 1-pyrrolidinyl, piperidino, 1-imidazolyl or 1,2,4-triazol-1-yl group as a substituent when m is 0 or, when m is 1, R.sup.5 is a lower alkoxycarbonyl group, a carboxyl group, a hydroxyl group, a group of the formula --C(.dbd.O)--N(R.sup.9)--R.sup.10 in which R.sup.9 and R.sup.10 are the same or different and each is a hydrogen atom, a lower alkyl group, a cycloalkyl group which may optionally have a benzene ring fused or condensed thereto, a phenyl group, a phenyl-lower alkyl group or a lower alkylsulfonyl group or R.sup.9 and R.sup.10 are bound to each other either directly or via an oxygen or sulfur atom to form, together with the adjacent nitrogen atom, a heterocyclic group which may optionally be substituted with a lower alkoxycarbonyl or carboxyl group, a group of the formula --CH.sub.2 --N(R.sup.11)--R.sup.12 in which R.sup.11 and R.sup.12 are the same or different and each is a hydrogen atom, a lower alkyl group, a cycloalkyl group which may optionally have a benzene ring condensed thereto, a phenyl group, a phenyl-lower alkyl group or a lower alkanoyl group or R.sup.11 and R.sup.12 are bound to each other either directly or via an oxygen or sulfur atom to form, together with the adjacent nitrogen atom, a heterocyclic group which may optionally be substituted with a lower alkoxycarbonyl or carboxyl group, a group of the formula --OR.sup.13 in which R.sup.13 is a lower alkylcarbamoylphenyl group, a lower alkylaminomethylphenyl group, a lower alkylaminomethylpenyl group, a 1-pyrrolidinylcarbonylphenyl group, a 1-pyrrolidinylmethylphenyl group, a 2-di-lower alkylaminoethyl group or a 2-hydroxyl-2-lower alkylaminoethyl group or a phenyl group which may optionally have a hydroxyl, lower alkoxy, 1-pyrrolidinylcarbonyl or 1-pyrrolidinylmethyl group as a substituent, and x is an integer of 0 to 2.
Dependencies are inferred from the claim text.