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公开(公告)号:ES2661444T3
公开(公告)日:2018-04-02
申请号:ES11878563
申请日:2011-12-28
Applicant: FUJIFILM CORP
Inventor: FUJIWARA HIDEYASU , MIZUMOTO SHINSUKE , KUBO YOHEI , NAKATA HIYOKU , HAGIWARA SHINJI , BABA YASUTAKA , TAMURA TAKASHI , KUNIYOSHI HIDENOBU , MASHIKO TOMOYUKI , YAMAMOTO MARI
IPC: C07D213/82 , A61K31/4439 , A61K31/455 , A61K31/506 , A61K31/5377 , A61P7/00 , A61P29/00 , A61P43/00 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/12 , C07D471/04
Abstract: Un derivado de nicotinamida que es: 6-(((1R,2S)-2-aminociclohexil)amino)-2-((3-(dimetilamino)-1-metil-1H-indazol-5-il)amino)-5-fluoronicotinamida; 6-(((1R,2S)-2-amino-1-ciclobutilpropil)amino)-5-fluoro-2-((1-metil-1H-indazol-6-il)amino)nicotinamida; 6-(((2R,3S)-3-aminopentan-2-il)amino)-2-((1-etil-1H-indazol-4-il)amino)-5-fluoronicotinamida; 6-(((3R,4S)-4-aminohexan-3-il)amino)-2-((1-etil-1H-indazol-4-il)amino)-5-fluoronicotinamida; 6-(((2S,3R)-2-amino-5-metilhexan-3-il)amino)-2-((1-etil-1H-indazol-6-il)amino)-5-fluoronicotinamida; 10 6-(((1R,2S)-2-amino-1-ciclobutilpropil)amino)-5-fluoro-2-((6-metoxi-5-(2H-1,2,3-triazol-2-il)piridin-3- il)amino)nicotinamida; 6-(((2S,3R)-2-amino-5-metilhexan-3-il)amino)-5-fluoro-2-((1-metil-1H-indazol-4-il)amino)nicotinamida; 6-(((2S,3S)-3-amino-1-metoxibutan-2-il)amino)-2-((3-(dimetilamino)-1-metil-1H-indazol-5-il)amino)-5- fluoronicotinamida; 6-(((2S,3S)-3-amino-1-metoxibutan-2-il)amino)-5-fluoro-2-((3-metoxi-1-metil-1H-indazol-5-il)amino)nicotinamida; 6-(((1R,2S)-2-aminociclohexil)amino)-5-fluoro-2-((3-metoxi-1-(2-metoxietil)-1H-indazol-5-il)amino)nicotinamida; (R)-6-((1-amino-4-metilpentan-2-il)amino)-5-fluoro-2-((3-metoxi-1-(2-metoxietil)-1H-indazol-5- il)amino)nicotinamida; 6-(((2S,3R)-2-aminopentan-3-il)amino)-5-fluoro-2-((3-metoxi-1-(2-metoxietil)-1H-indazol-5-il)amino)nicotinamida; 6-(((2S,3R)-2-aminohexan-3-il)amino)-5-fluoro-2-((3-metoxi-1-(2-metoxietil)-1H-indazol-5-il)amino)nicotinamida; 6-(((2S,3R)-2-amino-5-metilhexan-3-il)amino)-5-fluoro-2-((3-metoxi-1-(2-metoxietil)-1H-indazol-5- il)amino)nicotinamida; 6-(((1R,2S)-2-aminociclohexil)amino)-2-((3-(dimetilamino)-2-metil-2H-indazol-5-il)amino)-5-fluoronicotinamida; (R)-6-((1-amino-4-metilpentan-2-il)amino)-5-fluoro-2-((1-(2-metoxietil)-3-metil-1H-indazol-5-il)amino)nicotinamida; 6-(((2S,3R)-2-aminopentan-3-il)amino)-5-fluoro-2-((1-(2-metoxietil)-3-metil-1H-indazol-5-il)amino)nicotinamida; 6-(((2S,3R)-2-aminohexan-3-il)amino)-5-fluoro-2-((1-(2-metoxietil)-3-metil-1H-indazol-5-il)amino)nicotinamida; 6-(((1R,2S)-2-amino-1-ciclopropilpropil)amino)-5-fluoro-2-((1-(2-metoxietil)-3-metil-1H-indazol-5- il)amino)nicotinamida; 6-(((2S,3R)-2-amino-5-metilhexan-3-il)amino)-5-fluoro-2-((1-(2-metoxietil)-3-metil-1H-indazol-5- il)amino)nicotinamida; (R)-6-((1-amino-4-metilpentan-2-il)amino)-2-((1-(2,2-difluoroetil)-3-metil-1H-indazol-5-il)amino)-5- fluoronicotinamida; 6-(((2S,3R)-2-aminohexan-3-il)amino)-2-((1-(2,2-difluoroetil)-3-metil-1H-indazol-5-il)amino)-5-fluoronicotinamida; 6-(((2S,3S)-3-amino-1-metoxibutan-2-il)amino)-2-((1-(2,2-difluoroetil)-3-metil-1H-indazol-5-il)amino)-5- fluoronicotinamida; 6-(((2S,3R)-2-aminopentan-3-il)amino)-2-((7-cloro-1-metil-1H-indazol-5-il)amino)-5-fluoronicotinamida; 6-(((2S,3S)-3-amino-1-metoxibutan-2-il)amino)-2-((7-cloro-1-metil-1H-indazol-5-il)amino)-5-fluoronicotinamida; 6-(((2S,3R)-2-amino-5-metilhexan-3-il)amino)-2-((3-(dimetilamino)-2-metil-2H-indazol-5-il)amino)-5- fluoronicotinamida; 6-(((1R,2S)-2-aminociclohexil)amino)-5-fluoro-2-((7-fluoro-3-metoxi-1-metil-1H-indazol-5-il)amino)nicotinamida; (R)-6-((1-amino-4-metilpentan-2-il)amino)-5-fluoro-2-((7-fluoro-3-metoxi-1-metil-1H-indazol-5- il)amino)nicotinamida; 6-(((2S,3R)-2-aminopentan-3-il)amino)-5-fluoro-2-((7-fluoro-3-metoxi-1-metil-1H-indazol-5-il)amino)nicotinamida; 6-(((2S,3R)-2-aminohexan-3-il)amino)-5-fluoro-2-((7-fluoro-3-metoxi-1-metil-1H-indazol-5-il)amino)nicotinamida; 6-(((1R,2S)-2-amino-1-ciclopropilpropil)amino)-5-fluoro-2-((7-fluoro-3-metoxi-1-metil-1H-indazol-5- il)amino)nicotinamida; 6-(((2S,3R)-2-aminoheptan-3-il)amino)-5-fluoro-2-((7-fluoro-3-metoxi-1-metil-1H-indazol-5-il)amino)nicotinamida; 6-(((2S,3R)-2-amino-5-metilhexan-3-il)amino)-5-fluoro-2-((7-fluoro-3-metoxi-1-metil-1H-indazol-5- il)amino)nicotinamida; 6-(((2R,3S)-3-amino-1-ciclopropilbutan-2-il)amino)-5-fluoro-2-((7-fluoro-3-metoxi-1-metil-1H-indazol-5- il)amino)nicotinamida; 6-(((1R,2S)-2-amino-1-ciclobutilpropil)amino)-5-fluoro-2-((7-fluoro-3-metoxi-1-metil-1H-indazol-5- il)amino)nicotinamida; 6-(((2S,3S)-3-amino-1-metoxibutan-2-il)amino)-5-fluoro-2-((7-fluoro-3-metoxi-1-metil-1H-indazol-5- il)amino)nicotinamida; 6-(((3R,4S)-4-aminohexan-3-il)amino)-5-fluoro-2-((7-fluoro-3-metoxi-1-metil-1H-indazol-5-il)amino)nicotinamida; 6-(((1R,2S)-2-aminociclohexil)amino)-2-((3-(difluorometoxi)-1-metil-1H-indazol-5-il)amino)-5-fluoronicotinamida; 6-(((2S,3R)-2-aminopentan-3-il)amino)-2-((5,6-dimetilpiridin-3-il)amino)-5-fluoronicotinamida; 6-(((2S,3R)-2-aminopentan-3-il)amino)-2-((3-(difluorometoxi)-1-metil-1H-indazol-5-il)amino)-5-fluoronicotinamida; 6-(((1R,2S)-2-amino-1-ciclopropilpropil)amino)-2-((3-(difluorometoxi)-1-metil-1H-indazol-5-il)amino)-5- fluoronicotinamida; 6-(((2S,3R)-2-amino-5-metilhexan-3-il)amino)-2-((3-(difluorometoxi)-1-metil-1H-indazol-5-il)amino)-5- fluoronicotinamida; 6-(((2S,3S)-3-amino-1-metoxibutan-2-il)amino)-2-((3-(difluorometoxi)-1-metil-1H-indazol-5-il)amino)-5- fluoronicotinamida; 6-(((1R,2S)-2-aminociclohexil)amino)-2-((3-(difluorometoxi)-1-(2-metoxietil)-1H-indazol-5-il)amino)-5- fluoronicotinamida; 6-(((2S,3R)-2-aminopentan-3-il)amino)-2-((3-(difluorometoxi)-1-(2-metoxietil)-1H-indazol-5-il)amino)-5- fluoronicotinamida; 6-(((1R,2S)-2-amino-1-ciclopropilpropil)amino)-2-((3-(difluorometoxi)-1-(2-metoxietil)-1H-indazol-5-il)amino)-5-fluoronicotinamida; 6-(((2S,3R)-2-amino-5-metilhexan-3-il)amino)-2-((3-(difluorometoxi)-1-(2-metoxietil)-1H-indazol-5-il)amino)-5- fluoronicotinamida; 6-(((2S,3S)-3-amino-1-metoxibutan-2-il)amino)-2-((3-(difluorometoxi)-1-(2-metoxietil)-1H-indazol-5-il)amino)-5- fluoronicotinamida;
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公开(公告)号:NZ603837A
公开(公告)日:2014-01-31
申请号:NZ60383711
申请日:2011-06-30
Applicant: FUJIFILM CORP
Inventor: KURIHARA HIDEKI , KUBO YOHEI , TAMURA TAKASHI , YAMAMOTO MARI , SATO YUICHIRO , FUJIWARA HIDEYASU , HAGIWARA SHINJI , NAKATA HIYOKU , SATO KIMIHIKO , MIZUMOTO SHINSUKE , BABA YASUTAKA , KUNIYOSHI HIDENOBU
IPC: C07D213/82 , A61K31/44 , A61K31/443 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/4709 , A61K31/496 , A61K31/498 , A61K31/4985 , A61K31/506 , A61K31/517 , A61K31/5377 , A61K31/5383 , A61P7/00 , A61P29/00 , A61P37/00 , A61P43/00 , C07D215/40 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D491/048 , C07D491/056 , C07D491/107 , C07D498/04 , C07D513/04
Abstract: 603837 Disclosed herein is a nicotinamide derivative represented by the formula (I) or a salt thereof, wherein the variables are defined in the specification, and a pharmaceutical composition comprising said derivative for use in the treat ment of a Syk-related disease, such as rheumatism and idiopathic thrombocytopenic purpura. Embodiments of the derivative include the following: 6-(cis-2-aminocyclohexylamino)-5-fluoro-2-((8(methylsulphonamide)quinolin-3-yl)amino)nicotinamide, (R)-6-((1-aminobutan-2-yl)amino)-5-fluoro-2-((quinolin-6-yl)amino)nicotinamide, 6-((1R,2S)-2-aminocyclohexylamino)-5-fluoro-2-((isoquinolin-4-yl)amino)nicotinamide, and 5-((6-(cis-2-aminocyclohexylamino)-3-carbamoy1-5-fluoropyridin-2-yl)amino)-N-benzyl-1H-indole-2-carboxamide.
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公开(公告)号:HK1181762A1
公开(公告)日:2013-11-15
申请号:HK13109009
申请日:2013-08-01
Applicant: FUJIFILM CORP
Inventor: FUJIWARA HIDEYASU , SATO KIMIHIKO , MIZUMOTO SHINSUKE , SATO YUICHIRO , KURIHARA HIDEKI , KUBO YOHEI , NAKATA HIYOKU , BABA YASUTAKA , TAMURA TAKASHI , KUNIYOSHI HIDENOBU , HAGIWARA SHINJI , YAMAMOTO MARI
IPC: C07D20060101 , A61K20060101 , A61P20060101
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公开(公告)号:CA2803842C
公开(公告)日:2020-01-07
申请号:CA2803842
申请日:2011-06-30
Applicant: FUJIFILM CORP
Inventor: FUJIWARA HIDEYASU , SATO KIMIHIKO , MIZUMOTO SHINSUKE , SATO YUICHIRO , KURIHARA HIDEKI , KUBO YOHEI , NAKATA HIYOKU , BABA YASUTAKA , TAMURA TAKASHI , KUNIYOSHI HIDENOBU , HAGIWARA SHINJI , YAMAMOTO MARI
IPC: C07D213/82 , A61K31/44 , A61K31/443 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/4709 , A61K31/496 , A61K31/498 , A61K31/4985 , A61K31/506 , A61K31/517 , A61K31/5377 , A61K31/5383 , A61P7/00 , A61P29/00 , A61P37/00 , A61P43/00 , C07D215/40 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D491/048 , C07D491/056 , C07D491/107 , C07D498/04 , C07D513/04
Abstract: An object of the present invention is to provide to a compound and a pharmaceutical composition, which have excellent Syk-inhibitory activity. The present invention provides a nicotinamide derivative represented by the folio wing formula (I) (wherein R1 represents a halogen atom; R2 represents a C1-12 alkyl group, a C2-12 alkenyl group, a C2-12 alkynyl group, a C3-8 cycloalkyl group, an aryl group, an ar-C1-6, alkyl group or a heterocyclic group, each optionally having at least one substituent; R3 represents an aryl group or a heterocyclic group each optionally having at least one substituent; and R4 and R5 each independently represent a hydrogen atom) or a salt thereof, and a pharmaceutical composition for use in the treatment of a Syk-related disease which comprises the nicotinamide derivative or a salt thereof.
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公开(公告)号:RU2669806C1
公开(公告)日:2018-10-16
申请号:RU2017114338
申请日:2015-11-02
Applicant: FUJIFILM CORP
Inventor: KUNIYOSHI HIDENOBU , NAKAGAWA DAISUKE , MATSUMOTO TAKUYA , YOSHIMITSU YUJI
IPC: C07H19/10 , A61K31/7068 , A61P35/00 , A61P35/02
Abstract: Настоящееизобретениеотноситсяк производномутионуклеозида, представленномуобщейформулой [1]:, гдев R, Rи Rимеютзначенияуказанныев формулеизобретения, илиегосоль. Такжепредоставленафармацевтическаякомпозициядляпримененияприлеченииопухоли, содержащаяэффективноеколичествоуказанноговышепроизводноготионуклеозидаилиегосоли. Техническийрезультат– предоставлениепроизводноготионуклеозида, проявляющегопревосходныйэффектингибированияростагемцитабин-резистентныхклеток, ифармацевтическойкомпозиции, егосодержащей, проявляющейпревосходнуюлекарственнуюэффективностьпротивопухоли, котораяприобреларезистентностьк гемцитабину. 2 н. и 5 з.п. ф-лы, 24 табл., 55 пр.
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公开(公告)号:DK2799431T3
公开(公告)日:2018-03-26
申请号:DK11878563
申请日:2011-12-28
Applicant: FUJIFILM CORP
Inventor: FUJIWARA HIDEYASU , MIZUMOTO SHINSUKE , KUBO YOHEI , NAKATA HIYOKU , HAGIWARA SHINJI , BABA YASUTAKA , TAMURA TAKASHI , KUNIYOSHI HIDENOBU , MASHIKO TOMOYUKI , YAMAMOTO MARI
IPC: C07D213/82 , A61K31/4439 , A61K31/455 , A61K31/506 , A61K31/5377 , A61P7/00 , A61P29/00 , A61P43/00 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/12 , C07D471/04
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公开(公告)号:SG186877A1
公开(公告)日:2013-02-28
申请号:SG2012096632
申请日:2011-06-30
Applicant: FUJIFILM CORP
Inventor: FUJIWARA HIDEYASU , SATO KIMIHIKO , MIZUMOTO SHINSUKE , SATO YUICHIRO , KURIHARA HIDEKI , KUBO YOHEI , NAKATA HIYOKU , BABA YASUTAKA , TAMURA TAKASHI , KUNIYOSHI HIDENOBU , HAGIWARA SHINJI , YAMAMOTO MARI
Abstract: An object of the present invention is to provide to a compound and a pharmaceutical composition, which have excellent Syk-inhibitory activity. Th e present invention provides a nicotinamide derivative represented by the folio wing formula (I) (wherein RI represents a halogen atom; R2 represents a C1.12 alkyl group, a C2-I2 alkenyl group, a C2.12 alkynyl group, a C3-8 cycloalkyl g roup, an aryl group, an ar-C1_6 alkyl group or a heterocyclic group, each opti onally having at least one substituent; R3 represents an aryl group or a hetero cyclic group each optionally having at least one substituent; and R4 and R5 e ach independently represent a hydrogen atom; and R2 and R4 may form a cyclic amino group optionally having at least one substituent together with the ni trogen atom to which they bind) or a salt thereof, and a pharmaceutical comp osition for use in the treatment of a Syk-related disease which comprises the nicotinamide derivative or a salt thereof.
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公开(公告)号:AU2011272198A1
公开(公告)日:2013-02-07
申请号:AU2011272198
申请日:2011-06-30
Applicant: FUJIFILM CORP
Inventor: FUJIWARA HIDEYASU , SATO KIMIHIKO , MIZUMOTO SHINSUKE , SATO YUICHIRO , KURIHARA HIDEKI , KUBO YOHEI , NAKATA HIYOKU , BABA YASUTAKA , TAMURA TAKASHI , KUNIYOSHI HIDENOBU , HAGIWARA SHINJI , YAMAMOTO MARI
IPC: C07D213/82 , A61K31/44 , A61K31/443 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/4709 , A61K31/496 , A61K31/498 , A61K31/4985 , A61K31/506 , A61K31/517 , A61K31/5377 , A61K31/5383 , A61P7/00 , A61P29/00 , A61P37/00 , A61P43/00 , C07D215/40 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D491/048 , C07D491/056 , C07D491/107 , C07D498/04 , C07D513/04
Abstract: Provided are compounds having excellent Syk-inhibitory activity and pharmaceutical compositions. Specifically provided are: nicotinamide derivatives represented by general formula (I) or salts thereof; and pharmaceutical compositions for the treatment of Syk-related diseases, which contain the nicotinamide derivatives or the salts thereof. In general formula (I), R
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公开(公告)号:PL2799431T3
公开(公告)日:2018-07-31
申请号:PL11878563
申请日:2011-12-28
Applicant: FUJIFILM CORP
Inventor: FUJIWARA HIDEYASU , MIZUMOTO SHINSUKE , KUBO YOHEI , NAKATA HIYOKU , HAGIWARA SHINJI , BABA YASUTAKA , TAMURA TAKASHI , KUNIYOSHI HIDENOBU , MASHIKO TOMOYUKI , YAMAMOTO MARI
IPC: A61K31/4439 , C07D213/82 , A61K31/455 , A61K31/506 , A61K31/5377 , A61P7/00 , A61P29/00 , A61P43/00 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/12 , C07D471/04
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公开(公告)号:CA2861202C
公开(公告)日:2018-03-13
申请号:CA2861202
申请日:2011-12-28
Applicant: FUJIFILM CORP
Inventor: FUJIWARA HIDEYASU , MIZUMOTO SHINSUKE , KUBO YOHEI , NAKATA HIYOKU , HAGIWARA SHINJI , BABA YASUTAKA , TAMURA TAKASHI , KUNIYOSHI HIDENOBU , MASHIKO TOMOYUKI , YAMAMOTO MARI
IPC: C07D213/82 , A61K31/4439 , A61K31/455 , A61K31/506 , A61K31/5377 , A61P7/00 , A61P29/00 , A61P43/00 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/12 , C07D471/04
Abstract: The object of the present invention is to provide a compound and a pharmaceutical composition having excellent Syk inhibitory activity. According to the present invention, a nicotinamide derivative represented by the following formula (I) or a salt thereof is provided, (see formula I) wherein R1 is a substituent represented by the following formula (II-1), (III-1), or (IV- 1 ) (see formula II-1), (see formula III-1), (see formula IV-1.) (wherein R3, R4, R5, n, and XI have the same definitions as those described in the specification), and R2 is a pyridyl, indazolyl, phenyl, pyrazolopyridyl, benzisoxazolyl, pyrimidinyl, or quinolyl group, each of which optionally has at least one substituent.
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