Sankyo Company, Limited

Hitoshi Kurata

Koki Ishibashi

Hiroyoshi Horikoshi

Koichi Kojima

Takakazu Hamada

Takeshi Yamaguchi

Takahide Nishi

Katsuyoshi Nakajima

Tetsuya Fukazawa

Kazuhiro Ito

Takafumi Kohama

Ken Kitayama

Keita Kono

Method for treating an inflammatory disease

Cyclobutene derivatives, their preparation and their therapeutic uses

Compounds of the formula and quaternary ammonium ions thereof, wherein R.sup.1 and R.sup.2 are the same or different and are carbocyclic aryl or aromatic heterocyclic; A is methylene, carbonyl or sulfonyl; B is a single bond, C.sub.1 -C.sub.4 alkylene or C.sub.2 -C.sub.4, alkenylene; D is oxygen; E is C.sub.2 alkylene; G is C.sub.1 -C.sub.4 alkylene or C.sub.2 -C.sub.4 alkenylene; and L is --C(R.sup.4)(R.sup.5), wherein R.sup.4 and R.sup.5 together with the carbon atom to which they are attached represent a C.sub.5 -C.sub.10 cycloalkyl or a C.sub.5 -C.sub.10 heterocyclic. Especially preferred are compounds wherein L represents ##STR1## wherein J is a C.sub.1 -C.sub.6 alkylene; Ar is a ring carbocyclic or aromatic heterocyclic and S*.fwdarw.O is a sulfoxide in which the sulfur atom is in the 5-configuration. The compounds have tachykinin receptor antagonist activity and exhibit an activity against both the NK.sub.1 and NK.sub.2 receptors.

Heterocyclic compounds having tachykinin receptor antagonist activity

Compounds of formula (I): ##STR1## �wherein: R.sup.1 is hydrogen, alkyl, aryl-substituted alkyl or aromatic heterocyclic-substituted alkyl; R.sup.2 is: aryl-substituted alkyl, aromatic heterocyclic-substituted alkyl or diarylamino; and R.sup.3 is carboxy or a group of formula --CONHSO.sub.2 R.sup.4 wherein R.sup.4 is alkyl!; and pharmaceutically acceptable salts and esters thereof have valuable 5.alpha.-reductase inhibitory activity and can thus be used for the treatment and prophylaxis of, inter alia, prostatic hypertrophy as well as other disorders arising from excess levels of 5.alpha.-dihydrotestosterone.

Steroid derivatives for the treatment of prostatic hypertrophy, their

Method of making steroid derivatives for the treatment of prostatic

The invented compound ##STR1## is useful for the production of steroidal-17-amides that have 5.alpha.-reductase inhibitory activity.

Steroid derivatives

The invention includes compounds of formula (I): ##STR1## in which R.sup.1 is hydrogen, alkyl, aryl-substituted alkyl or aromatic heterocyclic-substituted alkyl; R.sup.2 is aryl-substituted alkyl, aromatic heterocyclic-substituted alkyl or diarylamino; and R.sup.3 is carboxy or a group of formula --CONHSO.sub.2 R.sup.4 wherein R.sup.4 is alkyl; and pharmaceutically acceptable salts and esters of the compounds. The compounds have valuable 5.alpha.-reductase inhibitory activity and can thus be used for the treatment and prophylaxis of, inter alia, prostatic hypertrophy as well as other disorders arising from excess levels of 5.alpha.-dihydro-testosterone.

Steroid derivatives for the treatment of prostatic hypertrophy their

Compounds of formula (I): ##STR1## (in which: R.sup.1 is a hydrogen atom, an unsubstituted alkyl group, an aryl-substituted alkyl group or a heterocyclic-substituted alkyl group; R.sup.2 is an aryl-substituted alkyl group, a heterocyclic-substituted alkyl group or a diarylamino group; R.sup.3 is a hydrogen atom, an unsubstituted alkyl group, an aryl-substituted alkyl group or an alkenyl group having from 3 to 6 carbon atoms; and each of the bonds represented by .alpha.-.beta. and .gamma.-.delta. is a carbon-carbon single bond or a carbon-carbon double bond;) and pharmaceutically acceptable salts and esters thereof are useful for the treatment and prophylaxis of prostatic hypertrophy. We also provide processes for their preparation.

Azasteroid compounds for the treatment of prostatic hypertrophy, their

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Tokyo, Japan

Hitoshi Kurata