Title:
N-PHENYLATED AMIDE AND UREA DERIVATIVES
Document Type and Number:
WIPO Patent Application WO/1996/003378
Kind Code:
A1
Abstract:
Novel N-phenylated amide and urea derivatives represented by general formula (I) and salts thereof, which have excellent ACAT inhibitory activity and peroral absorbability and are useful as a remedy and/or a preventive for arteriosclerosis, wherein R1a represents C1-C12 alkyl or cycloalkyl-alkyl; R16 represents H or any of the groups defined above with respect to R1a; R2a, R2b and R2c represent each independently H, optionally protected OH, nitro, C1-C12 alkyl, optionally mono- to pentafluorinated C1-C4 alkyl, alkoxy, halogeno, optionally C1-C4-alkylated mono- or dialkylamino, or five- or six-membered nitrogenous saturated heterocycle, or alternatively adjacent groups R2a and R2b are combined together to form -O-(CH2)m-O- (m being an integer of 1 to 3); R3 represents C1-C6 alkyl; R4 represents A1-R5 (A1 being C1-C6 alkylene or C3-C5 alkenylene; and R5 being a heterocyclic group selected from among those belonging to the following group 'alpha' and optionally substituted by halogeno, C1-C4 alkyl or C1-C4 hydroxyalkyl) or A2-X-A3-R5 (A2 being C1-C6 alkylene or C3-C5 alkenylene; X being O, S, NH, C1-C4 alkylimino, sulfinyl or sulfonyl; A3 being a single bond, C1-C6 alkylene or C3-C5 alkenylene; and R5 being as defined above, provided that the total number of the carbon atoms of A2 and A3 is 1 to 8 and that when A3 represents a single bond, the heterocyclic group R5 is bonded to X at the ring carbon atom); and n represents 0 or 1. Group 'alpha': imidazolyl, pyrazolyl, pyrazolidinyl, 1,2,4-triazolyl, tetrazolyl, morpholino, piperazinyl,2-pyridon-1-yl, 2-pyrimidinyl, pyridyl, pyrazinyl, 1,3,5-triazin-2-yl, benzimidazolyl, piperidinyl, pyrrolidinyl and azetidinyl groups.
Inventors:
YOSHIDA AKIRA (JP)
KOGEN HIROSHI (JP)
HAYAKAWA ICHIRO (JP)
ODA KOZO (JP)
KASAI TAKASHI (JP)
SIMADA KOUSEI (JP)
YOSHIDA YUMI (JP)
ISHIHARA SADAO (JP)
SAITO FUJIO (JP)
OHHATA YASUO (JP)
KOGA TEIICHIRO (JP)
KITAZAWA EIICHI (JP)
TOKUI TARO (JP)
KOGEN HIROSHI (JP)
HAYAKAWA ICHIRO (JP)
ODA KOZO (JP)
KASAI TAKASHI (JP)
SIMADA KOUSEI (JP)
YOSHIDA YUMI (JP)
ISHIHARA SADAO (JP)
SAITO FUJIO (JP)
OHHATA YASUO (JP)
KOGA TEIICHIRO (JP)
KITAZAWA EIICHI (JP)
TOKUI TARO (JP)
Application Number:
PCT/JP1995/001481
Publication Date:
February 08, 1996
Filing Date:
July 26, 1995
Export Citation:
Assignee:
SANKYO CO (JP)
YOSHIDA AKIRA (JP)
KOGEN HIROSHI (JP)
HAYAKAWA ICHIRO (JP)
ODA KOZO (JP)
KASAI TAKASHI (JP)
SIMADA KOSEI (JP)
YOSHIDA YUMI (JP)
ISHIHARA SADAO (JP)
SAITO FUJIO (JP)
OHHATA YASUO (JP)
KOGA TEIICHIRO (JP)
KITAZAWA EIICHI (JP)
TOKUI TARO (JP)
YOSHIDA AKIRA (JP)
KOGEN HIROSHI (JP)
HAYAKAWA ICHIRO (JP)
ODA KOZO (JP)
KASAI TAKASHI (JP)
SIMADA KOSEI (JP)
YOSHIDA YUMI (JP)
ISHIHARA SADAO (JP)
SAITO FUJIO (JP)
OHHATA YASUO (JP)
KOGA TEIICHIRO (JP)
KITAZAWA EIICHI (JP)
TOKUI TARO (JP)
International Classes:
C07D231/12; C07D233/54; C07D295/135; C07D317/58; C07D405/12; (IPC1-7): C07D213/40; C07D231/12; C07D233/62; C07D239/38; C07D239/42; C07D241/12; C07D253/02; C07D295/125; C07D319/12; C07D405/12
Foreign References:
| JPH06107655A | 1994-04-19 | |||
| JPH06122682A | 1994-05-06 |
Other References:
J. MED. CHEM., 1993, Vol. 36, No. 22, BHARAT K., TRIVEDI et al., "Inhibitors of ACAT", pages 3300-3307.
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