Sankyo Company, Limited

Daiichi Sankyo Company, Limited

Kousei Shimada

Akira Yoshida

Makoto Mori

Sadao Ishihara

Ichiro Hayakawa

Hiroshi Kogen

Teiichiro Koga

Eiichi Kitazawa

Takashi Kasai

Kozo Oda

Taro Tokui

Yoshitaka Nakamura

Yoshiyuki Onishi

Asuka Kawamura

Yuki Domon

Yukito Furuya

Naohisa Arakawa

An object of the present invention is to efficiently produce an optically active bicyclic compound. The optically active bicyclic compound is efficiently produced using an enzyme.

Optical resolution methods for bicyclic compounds using enzymes

It is intended to provide a bicyclic &#x3b3;-amino acid derivative having excellent activity as an &#x3b1;&#x3b4; ligand. The present invention provides a compound represented by the general formula (I): wherein R, R, R, R, R, R, R, R, and Rare a hydrogen atom or the like; and Ris a hydrogen atom, a halogen atom, a C1-C6 alkyl group, or the like.

Bicyclic &#x3b3;-amino acid derivative

Compounds of formula (I): ##STR1## wherein: R.sup.1 is alkyl; R.sup.2a, R.sup.2b, R.sup.2c and R.sup.2d are the same or different and each is hydrogen, optionally substituted alkyl or various other organic groups; R.sup.3 is alkyl; R.sup.4 is a group of formula (II), (III), (IV), (V), (VI), (VII), (VIII) or (IX): ##STR2## wherein: A.sup.1 is a single bond, alkylene or alkenylene; A.sup.2 is or alkenylene; A.sup.3 is a single bond, alkyleneor alkenylene; R.sup.5a and R.sup.5b are the same or different and each is hydrogen, alkyl or various other groups; R.sup.6 is alkyl or phenyl; R.sup.7 is hydrogen or alkyl; R.sup.8 is alkyl or various other groups; and n is 0 and pharmaceutically acceptable salts thereof have valuable inhibitory activity against acyl-CoA: cholesterol acyl transferase.

Urea derivatives having ACAT inhibitory activity, their preparation and

Compounds of formula (I): ##STR1## wherein: R.sup.1 is alkyl; R.sup.2a, R.sup.2b, R.sup.2c and R.sup.2d are the same or different and each is hydrogen, optionally substituted alkyl, --(C.dbd.O)--B.sup.1 (wherein B.sup.1 is hydrogen or alkyl), nitro, --NR.sup.c R.sup.d (wherein R.sup.c is hydrogen or alkyl and Rd is alkyl), hydroxy, protected hydroxy group, alkoxy, cyano, alkylthio, alkylsulfinyl, alkylsulfonyl or halogen; R.sup.3 is alkyl; R.sup.4 is a group of the formula (II) ##STR2## wherein A.sup.1 is a single bond, alkylene or alkenylene; R.sup.5a and R.sup.5b are the same or different and each is hydrogen, alkyl or --A.sup.4 R.sup.5.sub.c wherein A is a single bond, alkylene or alkenylene and R.sup.5.sub.c is alkoxy; and n is 0, and pharmaceutically acceptable salts thereof. Such compounds have valuable inhibitory activity against acyl-CoA (cholesterol acyl transferase).

Amide derivatives having ACAT inhibitory activity, their preparation and

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Tokyo, Japan

Kousei Shimada