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公开(公告)号：EP1698618A1
公开(公告)日：2006-09-06
申请号：EP04807929.7
申请日：2004-12-27
发明人： KOYANO, Hiroshi, c/o Chugai Seiyaku K. K. , SUDA, Atsushi, c/o Chugai Seiyaku K. K. , ASO, Kousuke, c/o Chugai Seiyaku K. K. , HADA, Kihito, c/o Chugai Seiyaku K. K. , ASAI, Miyuki, c/o Chugai Seiyaku K. K. , HASEGAWA, Masami, c/o Chugai Seiyaku K. K. , SATO, Yasuko, c/o Chugai Seiyaku K. K.
IPC分类号： C07C233/65 , C07C233/66 , C07C235/46 , C07C235/48 , C07C235/54 , C07C235/64 , C07C237/08 , C07C237/30 , C07C237/40 , C07C243/38 , C07C255/29 , C07C255/57 , C07C259/10 , C07C323/42 , C07C323/62 , C07D209/08 , C07D215/38 , C07D307/14 , C07D307/52 , C07D319/10 , A61K31/167
CPC分类号： C07C323/62 , C07C233/66 , C07C235/46 , C07C235/48 , C07C235/54 , C07C235/64 , C07C237/22 , C07C237/40 , C07C243/38 , C07C255/29 , C07C255/57 , C07C259/10 , C07C309/65 , C07C323/42 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07C2602/10 , C07D209/08 , C07D213/40 , C07D213/56 , C07D213/75 , C07D215/38 , C07D233/64 , C07D249/08 , C07D277/82 , C07D295/155 , C07D295/32 , C07D307/14 , C07D307/52 , C07D319/08 , C07D333/36
摘要： To provide compounds which have high angiogenesis inhibiting activity, and are useful as agents for effective treatment and prevention of diseases involving pathologic angiogenesis, for example, cancer and cancer metastasis, methods for producing the compounds, intermediate compounds useful for their production, and pharmaceutical compositions containing these compounds.
The present invention provides compounds of formula (II), or prodrugs thereof, or pharmaceutically acceptable salts of the compounds or the prodrugs, and pharmaceuticals, and pharmaceutical compositions containing these compounds:
whereA 1 is C-X 1 or N; Q 1 is -A 2 =A 3 -, or a heteroatom selected from -O-, -S-, and -N(R 10 )-; Q 2 is -A 4 =A 5 -, or a heteroatom selected from -O-, -S-, and -N(R 10 )-; provided that Q 1 and Q 2 are not heteroatoms at the same time; A 2 is C-X 2 or N, A 3 is C-X 3 or N, A 4 is C-X 4 or N, and A 5 is C-X 5 or N; Y is C 1-6 alkyl, C 3-9 cycloalkyl, C 2-7 alkenyl, C 2-7 alkynyl, C 1-6 alkoxy, C 2-7 alkenyloxy, C 2-7 alkynyloxy, or C 1-6 alkylthio; Z is a hydrogen atom, hydroxy, C 1-6 alkyl, C 3-9 cycloalkyl, or -NR 1 R 2 ; and L is selected from the formula:摘要翻译： 提供具有高血管生成抑制活性的化合物，并且可用作有效治疗和预防涉及病理血管发生的疾病，例如癌症和癌症转移的药物，用于制备化合物的方法，用于其制备的中间体化合物和药物组合物 含有这些化合物。 本发明提供式（II）化合物或其前药或化合物或前药的药学上可接受的盐，以及含有这些化合物的药物和药物组合物：其中A 1为C-X 1或N; Q 1是-A 2 = A 3 - 或选自-O - ， - S - 和-N（R 10） - 的杂原子。 Q 2是-A 4 = A 5 - 或选自-O - ， - S - 和-N（R 10） - 的杂原子。 条件是Q 1和Q 2不同时为杂原子; A 2是C-X 2或N，A 3是C-X 3或N，A 4是C-X 4或N，A 5是C-X 5或N; Y是C 1-6烷基，C 3-9环烷基，C 2-7烯基，C 2-7炔基，C 1-6烷氧基，C 2-7烯氧基，C 2-7炔氧基或C 1-6烷硫基 ; Z是氢原子，羟基，C 1-6烷基，C 3-9环烷基或-NR 1 R 2; L选自下式：
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公开(公告)号：EP1698618B1
公开(公告)日：2011-05-18
申请号：EP04807929.7
申请日：2004-12-27
发明人： KOYANO, Hiroshi, c/o Chugai Seiyaku K. K. , SUDA, Atsushi, c/o Chugai Seiyaku K. K. , ASO, Kousuke, c/o Chugai Seiyaku K. K. , HADA, Kihito, c/o Chugai Seiyaku K. K. , ASAI, Miyuki, , HASEGAWA, Masami, c/o Chugai Seiyaku K. K. , SATO, Yasuko, c/o Chugai Seiyaku K. K.
IPC分类号： C07C233/65 , C07C309/65 , C07C323/42 , C07C323/62 , C07D319/08 , C07D213/75 , C07D215/38 , C07D209/08 , C07D277/46 , A61P35/00
CPC分类号： C07C323/62 , C07C233/66 , C07C235/46 , C07C235/48 , C07C235/54 , C07C235/64 , C07C237/22 , C07C237/40 , C07C243/38 , C07C255/29 , C07C255/57 , C07C259/10 , C07C309/65 , C07C323/42 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07C2602/10 , C07D209/08 , C07D213/40 , C07D213/56 , C07D213/75 , C07D215/38 , C07D233/64 , C07D249/08 , C07D277/82 , C07D295/155 , C07D295/32 , C07D307/14 , C07D307/52 , C07D319/08 , C07D333/36
摘要： A compound which has high angiogenesis inhibitory activity and is useful in therapeutic and preventive drugs which are effective in diseases accompanied by diseased angiogenesis, e.g., cancers and the metastasis of cancers; a process for producing the compound; an intermediate useful in the production; and a medicine or medicinal composition containing the compound. The compound is one represented by the formula (II): a prodrug of the compound, or a pharmaceutically acceptable salt of either.
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