NOVEL AMIDRAZONE DERIVATIVES HAVING ANTIFUNGAL ACTIVITY

WIPO Patent Application WO/1998/058905

A1

Amidrazone derivatives of formula (I) useful for prevention or treatment of lupus mycosis attributable to fungi, such as Candida, Aspergillus, and Cryptococcus, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, wherein R?a¿ represents: (1) an optionally substituted monocyclic to tricyclic aromatic hydrocarbon, (2) an optionally substituted monocyclic to tricyclic saturated or unsaturated hetero ring containing one or more hetero atoms selected from N, O and S, (3) an optionally substituted and optionally cross-linked cycloalkyl, or (4) an optionally substituted and optionally cross-linked cycloalkenyl; R?b¿ represents (1) an optionally substituted monocyclic to tricyclic aromatic hydrocarbon or (2) an optionally substituted monocyclic to tricyclic saturated or unsaturated hetero ring containing one or more hetero atoms selected from N, O and S; <o>...</o> represents a single bond or a double bond; n is 1 to 8; A represents a bond or a lower alkylene optionally substituted by a lower alkyl; and X represents a bond, -CO-, -CO¿2?-, -CONR?g¿-, -COCONR?g1¿, -CH=CHCONR?g2¿-, -NR?g3¿, -NR?g4¿CO-, -NR?g5¿CO¿2?-, -NR?g6¿CONR?g7¿-, -O-, -OCO-, -OCONR?g8¿-, -OCH¿2?CONR?g9¿-, -S-, -SO-, -SO¿2?-, -SO¿2?NR?g10¿-, or -SO¿2?NR?g11¿CO-.

KAGEYAMA SHUNJI (JP)
KONTANI TORU (JP)
FUJII MASAHIRO (JP)
IGARASHI KIYOSHI (JP)
YAMAMOTO OSAMU (JP)

PCT/JP1998/002817

December 30, 1998

June 24, 1998

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YAMANOUCHI PHARMA CO LTD (JP)
KAGEYAMA SHUNJI (JP)
KONTANI TORU (JP)
FUJII MASAHIRO (JP)
IGARASHI KIYOSHI (JP)
YAMAMOTO OSAMU (JP)

C07C257/22; C07D207/416; C07D209/12; C07D209/88; C07D213/32; C07D213/64; C07D213/65; C07D213/77; C07D213/78; C07D213/82; C07D215/12; C07D215/14; C07D215/26; C07D215/46; C07D231/12; C07D237/14; C07D237/16; C07D237/22; C07D241/20; C07D241/24; C07D249/08; C07D263/58; C07D265/36; C07D277/38; C07D277/40; C07D277/42; C07D277/46; C07D279/16; C07D307/68; C07D311/14; C07D319/20; C07D333/38; C07D333/70; C07D401/12; C07D413/12; C07D473/08; C07D473/10; C07D487/04; C07D521/00; C07D207/40; (IPC1-7): C07C257/22; A61K31/155; A61K31/165; A61K31/17; A61K31/18; A61K31/215; A61K31/27; A61K31/275; A61K31/35; A61K31/38; A61K31/415; A61K31/425; A61K31/445; A61K31/47; A61K31/495; C07D211/40; C07D215/18; C07D215/26; C07D215/32; C07D231/12; C07D231/14; C07D249/08; C07D277/38; C07D277/44; C07D295/14; C07D295/18; C07D311/22; C07D333/38; C07D487/04

DE2436544A1

1975-02-13

FRASER J. K., ET AL.: "FORMATION OF OPTICALLY ACTIVE 1,2,4-TRIAZOLES FROM THE REACTIONS OF OPTICALLY ACTIVE N-ARYLMANDELAMIDRAZONES WITH TRIALKYL ORTHO ESTERS OR ALDEHYDES.", JOURNAL OF THE CHEMICAL SOCIETY, PERKIN TRANSACTIONS 1, ROYAL SOCIETY OF CHEMISTRY, GB, vol. 06., 1 January 1977 (1977-01-01), GB, pages 646 - 651., XP002912995, ISSN: 0300-922X, DOI: 10.1039/p19770000646
FRASER J. K., ET AL.: "FORMATION OF 1,2,4-TRIAZOLES FROM THE REACTIONS OF N-ARYLMANDELAMIDRAZONES WITH ALDEHYDES AND WITH TRIALKYL ORTHO ESTERS.", JOURNAL OF THE CHEMICAL SOCIETY, PERKIN TRANSACTIONS 1, ROYAL SOCIETY OF CHEMISTRY, GB, vol. 22., 1 January 1975 (1975-01-01), GB, pages 2280 - 2284., XP002912996, ISSN: 0300-922X, DOI: 10.1039/p19750002280

Nagai, Shozo (Patent & Information Dept., 17-1, Hasune 3-chom, Itabashi-ku Tokyo, JP)

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