Sankyo Company, Limited

Daiichi Sankyo Company, Limited

Kozo Oda

Akira Yoshida

Takahide Nishi

Hiroo Koyama

Koichi Hirai

Yuji Iwano

Teiichiro Koga

Takashi Kasai

Sadao Ishihara

Ichiro Hayakawa

Hiroshi Kogen

Eiichi Kitazawa

Kousei Shimada

Taro Tokui

Takahiro Yamaguchi

Kazuo Hasegawa

Naoki Terasaka

Kazuhiko Tamaki

Daisuke Nakai

Masakazu Nakadai

A superior LXR modulator is provided. A compound represented by the general formula (I): [wherein R: &#x2014;COR(wherein R: alkyl, optionally substituted alkoxy or optionally substituted amino); R: H, OH, alkoxy, optionally substituted amino, etc.; R: H, optionally substituted alkyl, cycloalkyl, optionally substituted alkoxy, optionally substituted amino, halogeno, etc.; Rand R: H, optionally substituted alkyl, halogeno, etc.; Rand R: H, alkyl; R: &#x2014;XR[wherein R: &#x2014;COR(wherein R: OH, optionally substituted alkoxy, optionally substituted amino, etc.), &#x2014;SOR(wherein R: optionally substituted alkyl, optionally substituted amino, etc.), tetrazol-5-yl, etc.; X: single bond, optionally substituted alkylene, etc.]; X: &#x2014;NH&#x2014;, &#x2014;O&#x2014;, &#x2014;S&#x2014;, etc.; Y: optionally substituted phenyl, optionally substituted 5- to 6-membered aromatic heterocyclyl; Y: optionally substituted aryl, optionally substituted heterocyclyl, etc.] and the like is provided.

Benzene compound having 2 or more substituents

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

A method for preparing compounds of formula (I): ##STR1## wherein: R.sup.1 is hydrogen or a hydroxy-protecting group; R.sup.2 is alkyl, alkoxy, halogen, optionally substituted phenyl or optionally substituted phenoxy; R.sup.3 is optionally substituted pyridyl, optionally substituted quinolyl or phenyl group which has a substituent of formula --CYNR.sup.5 R.sup.6, where Y is oxygen or sulfur, and R.sup.5 and R.sup.6 are each alkyl, aryl or aralkyl, or R.sup.5 and R.sup.6 and the nitrogen to which they are attached together form a heterocyclic group; R.sup.4 is hydrogen or an amino-protecting group; and Z is sulfur or oxygen. The process comprises reacting a compound of formula (II): ##STR2## in which R.sup.8, R.sup.9 and R.sup.10 are the same or different and each represents an alkyl group having from 1 to 4 carbon atoms or a phenyl group, with a compound of formula (III): ##STR3## in which R.sup.11 represents an acyloxy, alkylsulfonyl, arylsulfonyl, alkylsulfinyl or arylsulfinyl group.

Silyl enol ether alkylation process

A process for preparing a compound of formula (I'): ##STR1## comprising reacting a compound of formula (II'): ##STR2## with a compound of formula (III'):

Metal catalyzed displacement process

A compound of the formula ##STR1## in which: R.sup.1' is hydrogen or a carboxy-protecting group;

Carbapenem

Tricyclic heterocyclic compound

Compounds of formula (I): ##STR1## wherein: R.sup.1 is hydrogen or a hydroxy-protecting group; R.sup.2 is alkyl, alkoxy, halogen, optionally substituted phenyl or optionally substituted phenoxy; R.sup.3 is optionally substituted pyridyl, optionally substituted quinolyl or phenyl group which has a substituent of formula --CYNR.sup.5 R.sup.6, where Y is oxygen or sulfur, and R.sup.5 and R.sup.6 are each alkyl, aryl or aralkyl, or R.sup.5 and R.sup.6 and the nitrogen to which they are attached together form a heterocyclic group; is R.sup.4 hydrogen or an amino-protecting group; and Z is sulfur or oxygen; are valuable intermediates in the preparation of carbapenem compounds and retain a desirable configuration during conversion to such carbapenem compounds. Penem and carbapenem compounds having a group of formula --SA' are prepared from a corresponding compound having a substituted thio, sulfinyl or sulfonyl group at this position by reaction with a compound A'SH (where A' is an organic group) in the presence of a salt of a metal of Group II or III of the Periodic Table.

Azetidinone compounds useful in the preparation of carbapenem

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Tokyo, Japan

Kozo Oda