Substituted guanidine derivatives
AssigneeUbe Industries, Ltd.
InventorsKen-ichi Komori, Akishi Ninomiya, Shigeru Ushiyama, Masaru Shinohara, Koji Ito, Tetsuo Kawaguchi, Yasunori Tokunaga, Hiroyoshi Kawada, Haruka Yamada, Yusuke Shiraishi, Masahiro Kojima, Masaaki Ito, Tomio Kimura
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Abstract
The present invention provides a compound of general formula (I) (wherein, R1, X, p and q are as described in the present description and claims), or a pharmacologically acceptable salt thereof, and a pharmaceutical composition containing that compound.
Claims30
A compound of formula (I):
- wherein,
- R1 represents a hydrogen atom, C1-C7 acyl group, tri(C1-C4 alkyl)silyl group, tetrahydropyranyl group, triphenylmethyl group, optionally substituted C1-C6 alkyl group, optionally substituted C2-C6 alkenyl group, optionally substituted C3-C8 cycloalkyl group, optionally substituted C1-C6 alkoxy-C1-C6 alkyl group, —CONR11R12, optionally substituted heterocyclyl group, optionally substituted heterocyclyl-C1-C6 alkyl group, optionally substituted aryl group or optionally substituted C7-C16 aralkyl group, and
- X represents N or C—R2,
- wherein, R2 represents a hydrogen atom, halogen atom, optionally substituted C1-C6 alkyl group, optionally substituted C3-C8 cycloalkyl group, optionally substituted C1-C6 alkoxy group or cyano group,
- p and q, independently of each other, represent a natural number of 1 to 3, provided that the sum of p and q is a natural number of 2 to 4,
- wherein, the term “substituted” refers to being substituted with at least one substituent selected from the group consisting of a deuterium atom, halogen atom, C1-C6 alkyl group, C1-C6 alkoxy group, C1-C6 alkoxy-C1-C6 alkyl group, R13O-C1-C6 alkyl group, halo-C1-C6 alkyl group, C7-C16 aralkyl group, C1-C7 acyl group, cyano group, oxo group, —CONR11R12, —OR13, —COOR14, —NR15R16 and —S(O)nR17,
- R11 and R12 independently represent a hydrogen atom or C1-C6 alkyl group, R13 represents a hydrogen atom, C1-C7 acyl group, tri(C1-C4 alkyl)silyl group, tetrahydropyranyl group or triphenylmethyl group, or if two —OR13 groups are present and a 1,2- or 1,3-diol structure is formed, R13 can represent acetonide, R14 represents a hydrogen atom or C1-C6 alkyl group, R15 and R16 independently represent a hydrogen atom, C1-C6 alkyl group, C7-C16 aralkyl group, C1-C7 acyl group, —COOR14 or —S(O)nR17, R17 represents a C1-C6 alkyl group, and n represents 0, 1 or 2;
- or a pharmacologically acceptable salt thereof.
2-fluoro-3-{2-[3-(methoxyimino)azetidin-1-yl]pyrimidin-5-yl}benzyl carbamimidoylcarbamate or a pharmacologically acceptable salt thereof.
3-{2-[3-(ethoxyimino)azetidin-1-yl]pyrimidin-5-yl}-2-fluorobenzyl carbamimidoylcarbamate or a pharmacologically acceptable salt thereof.
2-fluoro-3-(2-{3-[(methoxy-d3)imino]azetidin-1-yl}pyrimidin-5-yl)benzyl carbamimidoylcarbamate or a pharmacologically acceptable salt thereof.
2-fluoro-3-(2-{3-[(2-fluoroethoxy)imino]azetidin-1-yl}pyrimidin-5-yl}benzyl carbamimidoylcarbamate or a pharmacologically acceptable salt thereof.
2-fluoro-3-{5-fluoro-6-[3-(methoxyimino)azetidin-1-yl]pyridin-3-yl}benzyl carbamimidoylcarbamate or a pharmacologically acceptable salt thereof.
2-fluoro-3-{5-fluoro-6-{3-[(methoxy-d3)imino]azetidin-1-yl}pyridine-3-yl}benzyl carbamimidoylcarbamate or a pharmacologically acceptable salt thereof.
3-(6-{3-[(3,4-dihydroxybutoxy)imino]azetidin-1-yl}-5-fluoropyridin-3-yl)-2-fluorobenzyl carbamimidoylcarbamate or a pharmacologically acceptable salt thereof.
2-fluoro-3-{5-fluoro-6-[3-{[hydroxyl-2-(hydroxymethyl)propoxy]imino}azetidin-1-yl]pyridin-3-yl}benzyl carbamimidoylcarbamate or a pharmacologically salt thereof.
2-fluoro-3-(2-{3-[(2-fluoro-3-hydroxypropoxy)imino]azetidin-1-yl}pyrimidin-5-yl)benzyl carbamimidoylcarbamate or a pharmacologically acceptable salt thereof.
3-[({1-[5-(3-{[(carbamimidoylcarbamoyl)oxy]methyl}-2-fluorophenyl)pyrimidin-2-yl]azetidin-3-ylidene}amino)oxy]cyclobutyl acetate or a pharmacologically acceptable salt thereof.
2-fluoro-3-(2-{3-[(3-hydroxycyclobutoxy)imino]azetidin-1-yl}pyrimidin-5-yl)benzyl carbamimidoylcarbamate or a pharmacologically acceptable salt thereof.
2-fluoro-3-{2-[3-({[1-(methylsulfonyl)azetidin-3-yl]oxy}imino)azetidin-1-yl]pyrimidin-5-yl}benzyl carbamimidoylcarbamate or a pharmacologically acceptable salt thereof.
2-fluoro-3-(2-{3-[(oxetan-3-yloxy)imino]azetidin-1-yl}pyrimidin-5-yl)benzyl carbamimidoylcarbamate or a pharmacologically acceptable salt thereof.
Dependencies are inferred from the claim text.