摘要:
The present invention provides a compound consisting of a moiety and a group chemically bonded to said moiety, wherein said moiety contains a compound having low activity following oral administration or its parent scaffold and said group has the following general formula (1): in which R1 represents a hydrogen atom, etc., R2 represents a C1-C7 halogenoalkyl group, etc., m represents an integer of 2 to 14, and n represents an integer of 2 to 7, or enantiomers of the compound, or hydrates or pharmaceutically acceptable salts of the compound or enantiomers thereof. The above compound is advantageous in pharmaceutical use because the group of general formula (1) allows compounds such as anti-estrogenic ones to show a significantly increased activity following oral administration when attached to the parent scaffolds of the compounds.
摘要:
The present invention provides a compound consisting of a moiety and a group chemically bonded to said moiety, wherein said moiety contains a compound having low activity following oral administration or its parent scaffold and said group has the following general formula (1): in which R1 represents a hydrogen atom, etc., R2 represents a C1–C7 halogenoalkyl group, etc., m represents an integer of 2 to 14, and n represents an integer of 2 to 7, or enantiomers of the compound, or hydrates or pharmaceutically acceptable salts of the compound or enantiomers thereof. The above compound is advantageous in pharmaceutical use because the group of general formula (1) allows compounds such as anti-estrogenic ones to show a significantly increased activity following oral administration when attached to the parent scaffolds of the compounds.
摘要:
The present invention provides a compound consisting of a moiety and a group chemically bonded to said moiety, wherein said moiety contains a compound having low activity following oral administration or its parent scaffold and said group has the following general formula (1): in which R1 represents a hydrogen atom, etc., R2 represents a C1-C7 halogenoalkyl group, etc., m represents an integer of 2 to 14, and n represents an integer of 2 to 7, or enantiomers of the compound, or hydrates or pharmaceutically acceptable salts of the compound or enantiomers thereof. The above compound is advantageous in pharmaceutical use because the group of general formula (1) allows compounds such as anti-estrogenic ones to show a significantly increased activity following oral administration when attached to the parent scaffolds of the compounds.
摘要翻译:本发明提供了由部分和化学键合到所述部分的基团组成的化合物,其中所述部分含有口服后具有低活性的化合物或其母体支架,所述基团具有以下通式(1):其中R R 1表示氢原子等,R 2表示C 1 -C 7卤代烷基等 m表示2〜14的整数,n表示2〜7的整数,或该化合物的对映异构体,或其化合物或其对映异构体的水合物或药学上可接受的盐。 上述化合物在药物用途中是有利的,因为通式(1)的基团允许化合物如抗雌激素的化合物在连接到化合物的母体支架上时在口服给药后显示出显着增加的活性。
摘要:
A compound having the following general formula (1): in which R1 represents an ethyl group, etc.; R2 represents a hydrogen atom, etc.; R3 represents a C1-C5 perhalogenoalkyl group, etc.; each of R4 and R5 independently represents a hydrogen atom, etc.; X represents an oxygen atom or a sulfur atom; m represents an integer of 2 to 14; and n represents an integer of 2 to 7; or an enantiomer of the compound, or a hydrate or a pharmaceutically acceptable salt of the compound or its enantiomer is advantageous in pharmaceutical use because of its anti-estrogenic activity.
摘要:
The present invention relates to 3-methyl-chromane or thiochromane derivatives, pharmaceutically acceptable salts, stereoisomers or hydrates thereof, and an anti-estrogenic pharmaceutical composition which comprises the above compound as an active component.
摘要:
The present invention provides a compound having the following general formula (1): in which R1 represents a hydrogen atom, etc.; R2 represents a C3-C3 perhalogenoalkyl group, etc.; each of R3 and R4 independently represents a hydrogen atom, etc.; X represents an oxygen atom or a sulfur atom; m represents an integer of 2 to 14; and n represents an integer of 0 to 8; or enantiomers of the compound, or hydrates or pharmaceutically acceptable salts of the compound or its enantiomers. The compound of general formula (1) is advantageous in pharmaceutical use because of its anti-estrogenic activity.
摘要翻译:本发明提供具有以下通式(1)的化合物:其中R 1表示氢原子等; R 2表示C 3 -C 3全卤代烷基等; R 3和R 4各自独立地表示氢原子等。 X表示氧原子或硫原子,m表示2〜14的整数, 和n表示0至8的整数;或化合物的对映异构体,或化合物或其对映异构体的水合物或药学上可接受的盐。 通式(1)的化合物由于其抗雌激素活性而在药物应用中是有利的。