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公开(公告)号：US07964623B2
公开(公告)日：2011-06-21
申请号：US12591353
申请日：2009-11-17
IPC分类号： A61K31/429 , C07D513/06
CPC分类号： C07D513/04 , C07D491/04 , C07D515/04
摘要： This invention relates to benzopyran derivatives of formula (I) or (II), or pharmaceutically acceptable salts thereof wherein R1 and R2 are independently of each other hydrogen atom, C1-6alkyl group or C6-14aryl group, R3 is hydrogen atom or C1-6alkylcarbonyloxy group, or together with R4 forms a bond, R4 is hydrogen atom, or together with R3 forms a bond, m is an integer of 0 to 4, n is an integer of 0 to 4, V is a single bond, CR7R8, NR9, O, S, SO or SO2, R5 is hydrogen atom or C1-6alkyl group, R6 is hydrogen atom, C1-6alkyl group, C3-8cycloalkyl group, C3-8cycloalkenyl group, amino group, C1-6alkylamino group, di-C1-6alkylamino group, C6-14arylamino group, C2-9heteroarylamino group, C6-14aryl group, C2-9heteroaryl group or C2-9heterocyclyl group, A is 5-, 6- or 7-member ring fused with benzene ring, as constituent atom of the ring, oxygen atom, nitrogen atom or sulfur atom may be contained in the number of 1 to 3 alone or in a combination thereof, the number of unsaturated bond in the ring is 1, 2 or 3 including an unsaturated bond of the benzene ring to be fused, carbon atoms constituting the ring may be carbonyl or thiocarbonyl. These compounds are useful as an anti-arrhythmic agent.
摘要翻译： 本发明涉及式（I）或（II）的苯并吡喃衍生物或其药学上可接受的盐，其中R1和R2彼此独立地为氢原子，C1-6烷基或C6-14芳基，R3为氢原子或C1- C 1-6烷基羰基氧基或与R 4一起形成键，R 4为氢原子，或与R 3一起形成键，m为0〜4的整数，n为0〜4的整数，V为单键，CR 7 R 8， NR9，O，S，SO或SO2，R5是氢原子或C1-6烷基，R6是氢原子，C1-6烷基，C3-8环烷基，C3-8环烯基，氨基，C1-6烷基氨基， C 1-6烷基氨基，C 6-14芳基氨基，C 2-9杂芳基氨基，C 6-14芳基，C 2-9杂芳基或C 2-9杂环基，A是与苯环稠合的5-，6-或7-元环作为构成原子 的环，氧原子，氮原子或硫原子可以单独或组合1〜3的数量包含在t中的不饱和键的数量 环是1,2或3，包括待稠合的苯环的不饱和键，构成环的碳原子可以是羰基或硫代羰基。 这些化合物可用作抗心律不齐剂。
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公开(公告)号：US5880301A
公开(公告)日：1999-03-09
申请号：US894520
申请日：1997-09-16
CPC分类号： B01J31/2295 , B01J31/2409 , B01J31/2414 , B01J31/2452 , C07F15/0066 , B01J2231/4272 , B01J2531/0205 , B01J2531/0266 , B01J2531/824 , B01J2531/842
摘要： The present invention provides a novel optically active bidentate phosphine ligand palladium complex of formula (I) or (II) which can be used for the preparation of optically active .beta.-hydroxyketones: ##STR1## �wherein Y.sup.- represents an anion pair which may form salt; X represents ##STR2## {wherein R.sup.1 represents hydrogen atom, C.sub.1-6 alkyl group, C.sub.1-6 alkoxyl group, cyano group, nitro group, halogen atom or phenyl group, etc.; m represents 1 or 2; when m is 2, two R.sup.1 s may be same or different}; andA and B each independently represents phenyl group or cyclohexyl group {said phenyl group and cyclohexyl group each is unsubstituted or substituted by R.sup.2 (R.sup.2 has the same meaning as defined in R.sup.1)}).
摘要翻译： PCT No.PCT / JP96 / 00418 Sec。 371日期：1997年9月16日 102（e）日期1997年9月16日PCT提交1996年2月23日PCT公布。 出版物WO96 / 26210 日期：1996年8月29日本发明提供了可用于制备光学活性β-羟基酮的式（I）或（II）的新型光学活性二齿膦配体钯络合物： （II）[其中Y-表示可形成盐的阴离子对; X代表原子，C 1-6烷基，C 1-6烷氧基，氰基，硝基，卤原子或苯基等; m表示1或2; 当m为2时，两个R1可以相同或不同}; A和B各自独立地表示苯基或环己基（所述苯基和环己基各自未被取代或被R 2取代（R 2具有与R 1中定义相同的含义）}）。
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13.发明授权α-amino acid derivatives and medicaments containing the same as an active ingredient 有权α-氨基酸衍生物和含有活性成分的药物公开(公告)号：US07879887B2
公开(公告)日：2011-02-01
申请号：US12306901
申请日：2007-06-29
申请人： Kazuhiko Ohrai , Michiaki Adachi , Koji Toyama , Takanori Shimizu , Keishi Hayashi , Masataka Minami , Yoshiyuki Suzuki , Masakazu Sugiyama , Masateru Ohta , Shojiro Kadono , Takuya Shiraishi , Haruhiko Sato , Yoshiaki Watanabe , Nobuya Ishii , Masahiro Sakaitani , Masami Hasegawa
发明人： Kazuhiko Ohrai , Michiaki Adachi , Koji Toyama , Takanori Shimizu , Keishi Hayashi , Masataka Minami , Yoshiyuki Suzuki , Masakazu Sugiyama , Masateru Ohta , Shojiro Kadono , Takuya Shiraishi , Haruhiko Sato , Yoshiaki Watanabe , Nobuya Ishii , Masahiro Sakaitani , Masami Hasegawa
IPC分类号： C07D513/04 , A61K31/429
CPC分类号： C07D513/04
摘要： The present invention provides novel α-amino acid derivatives of formula (1): (wherein, R1, R2, R3, R4, X and Y are as defined in the claims) or pharmaceutically acceptable salts, prodrugs or solvates thereof. The derivatives of formula (1) have βARK1 inhibitory activity and are useful for preventing or treating heart failure. Moreover, the derivatives of formula (1) also have antitumor activity, particularly dual inhibitory activity on Aurora kinase and CDK, and are useful for cell proliferative diseases such as cancer.
摘要翻译： 本发明提供新的式（1）的α-氨基酸衍生物：其中R1，R2，R3，R4，X和Y如权利要求中所定义）或其药学上可接受的盐，前药或溶剂合物。 式（1）的衍生物具有ARK1抑制活性，可用于预防或治疗心力衰竭。 此外，式（1）的衍生物还具有抗肿瘤活性，特别是对极光激酶和CDK的双重抑制活性，并且可用于细胞增殖性疾病如癌症。
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公开(公告)号：US20100069374A1
公开(公告)日：2010-03-18
申请号：US12591353
申请日：2009-11-17
IPC分类号： A61K31/542 , A61K31/5383 , A61K31/4985 , A61K31/519 , A61K31/436 , A61K31/429 , A61K31/424 , A61K31/4188 , A61K31/4162 , A61K31/407 , C07D513/04 , C07D498/04 , C07D491/052 , A61P9/06
CPC分类号： C07D513/04 , C07D491/04 , C07D515/04
摘要： This invention relates to benzopyran derivatives of formula (I) or (II), or pharmaceutically acceptable salts thereof wherein R1 and R2 are independently of each other hydrogen atom, C1-6alkyl group or C6-14aryl group, R3 is hydrogen atom or C1-6alkylcarbonyloxy group, or together with R4 forms a bond, R4 is hydrogen atom, or together with R3 forms a bond, m is an integer of 0 to 4, n is an integer of 0 to 4, V is a single bond, CR7R8, NR9, O, S, SO or SO2, R5 is hydrogen atom or C1-6alkyl group, R6 is hydrogen atom, C1-6alkyl group, C3-8cycloalkyl group, C3-8cycloalkenyl group, amino group, C1-6alkylamino group, di-C1-6alkylamino group, C6-14arylamino group, C2-9heteroarylamino group, C6-14aryl group, C2-9heteroaryl group or C2-9heterocyclyl group, A is 5-, 6- or 7-member ring fused with benzene ring, as constituent atom of the ring, oxygen atom, nitrogen atom or sulfur atom may be contained in the number of 1 to 3 alone or in a combination thereof, the number of unsaturated bond in the ring is 1, 2 or 3 including an unsaturated bond of the benzene ring to be fused, carbon atoms constituting the ring may be carbonyl or thiocarbonyl. These compounds are useful as an anti-arrhythmic agent.
摘要翻译： 本发明涉及式（I）或（II）的苯并吡喃衍生物或其药学上可接受的盐，其中R1和R2彼此独立地为氢原子，C1-6烷基或C6-14芳基，R3为氢原子或C1- C 1-6烷基羰基氧基或与R 4一起形成键，R 4为氢原子，或与R 3一起形成键，m为0〜4的整数，n为0〜4的整数，V为单键，CR 7 R 8， NR9，O，S，SO或SO2，R5是氢原子或C1-6烷基，R6是氢原子，C1-6烷基，C3-8环烷基，C3-8环烯基，氨基，C1-6烷基氨基， C 1-6烷基氨基，C 6-14芳基氨基，C 2-9杂芳基氨基，C 6-14芳基，C 2-9杂芳基或C 2-9杂环基，A是与苯环稠合的5-，6-或7-元环作为构成原子 的环，氧原子，氮原子或硫原子可以单独或组合1〜3的数量包含在t中的不饱和键的数量 环是1,2或3，包括待稠合的苯环的不饱和键，构成环的碳原子可以是羰基或硫代羰基。 这些化合物可用作抗心律不齐剂。
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公开(公告)号：US20080004262A1
公开(公告)日：2008-01-03
申请号：US10590975
申请日：2005-03-23
IPC分类号： A61K31/436 , A61K31/403 , A61K31/495 , A61K31/517 , A61K31/538 , A61P9/06 , C07D209/56 , C07D221/02 , C07D235/02 , C07D241/36 , C07D265/38 , C07D515/12
CPC分类号： C07D513/04 , C07D491/04 , C07D515/04
摘要： This invention relates to benzopyran derivatives of formula (I) or (II), or pharmaceutically acceptable salts thereof wherein R1 and R2 are independently of each other hydrogen atom, C1-6alkyl group or C6-14aryl group, R3 is hydrogen atom or C1-6alkylcarbonyloxy group, or together with R4 forms a bond, R4 is hydrogen atom, or together with R3 forms a bond, m is an integer of 0 to 4, n is an integer of 0 to 4, V is a single bond, CR7R8, NR9, O, S, SO or SO2, R5 is hydrogen atom or C1-6alkyl group, R6 is hydrogen atom, C1-6alkyl group, C3-8cycloalkyl group, C3-8cycloalkenyl group, amino group, C1-6alkylamino group, di-C1-6alkylamino group, C6-14arylamino group, C2-9heteroarylamino group, C6-14aryl group, C2-9heteroaryl group or C2-9heterocyclyl group, A is 5-, 6- or 7-member ring fused with benzene ring, as constituent atom of the ring, oxygen atom, nitrogen atom or sulfur atom may be contained in the number of 1 to 3 alone or in a combination thereof, the number of unsaturated bond in the ring is 1, 2 or 3 including an unsaturated bond of the benzene ring to be fused, carbon atoms constituting the ring may be carbonyl or thiocarbonyl. These compounds are useful as an anti-arrhythmic agent.
摘要翻译： 本发明涉及式（I）或（II）的苯并吡喃衍生物或其药学上可接受的盐，其中R 1和R 2彼此独立地为氢原子，C C 1-6烷基或C 6-14芳基，R 3是氢原子或C 1-6 >烷基羰氧基，或与R 4连接形成键，R 4是氢原子，或与R 3 3一起形成键，m 为0〜4的整数，n为0〜4的整数，V为单键，CR 7，R 8，NR 9， >，O，S，SO或SO 2，R 5是氢原子或C 1-6烷基，R 6 C 1-6烷基，C 3-8环烷基，C 3-8环烯基，C 3-8环烷基，C 3-6环烷基， 氨基，C 1-6烷基氨基，二-C 1-6烷基氨基，C 6-14芳基氨基，C 2-9个杂芳基氨基，C 6-14-14芳基，C 2-9 - 杂芳基 A或C 2-9杂环基，A是与苯环稠合的5-，6-或7-元环，作为环的构成原子，氧原子，氮原子或硫原子可以 单独或以其组合存在1〜3的数量，环中的不饱和键数为1,2或3，包括要被稠合的苯环的不饱和键，构成环的碳原子可以是羰基 或硫代羰基。 这些化合物可用作抗心律不齐剂。
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公开(公告)号：US07652008B2
公开(公告)日：2010-01-26
申请号：US10590975
申请日：2005-03-23
IPC分类号： A61K31/436 , A61K31/519 , A61K31/4365 , C07D265/38 , C07D491/06 , C07D498/06
CPC分类号： C07D513/04 , C07D491/04 , C07D515/04
摘要： This invention relates to benzopyran derivatives of formula (I) or (II), or pharmaceutically acceptable salts thereof wherein R1 and R2 are independently of each other hydrogen atom, C1-6alkyl group or C6-14aryl group, R3 is hydrogen atom or C1-6alkylcarbonyloxy group, or together with R4 forms a bond, R4 is hydrogen atom, or together with R3 forms a bond, m is an integer of 0 to 4, n is an integer of 0 to 4, V is a single bond, CR7R8, NR9, O, S, SO or SO2, R5 is hydrogen atom or C1-6alkyl group, R6 is hydrogen atom, C1-6alkyl group, C3-8cycloalkyl group, C3-8cycloalkenyl group, amino group, C1-6alkylamino group, di-C1-6alkylamino group, C6-14arylamino group, C2-9heteroarylamino group, C6-14aryl group, C2-9heteroaryl group or C2-9heterocyclyl group, A is 5-, 6- or 7-member ring fused with benzene ring, as constituent atom of the ring, oxygen atom, nitrogen atom or sulfur atom may be contained in the number of 1 to 3 alone or in a combination thereof, the number of unsaturated bond in the ring is 1, 2 or 3 including an unsaturated bond of the benzene ring to be fused, carbon atoms constituting the ring may be carbonyl or thiocarbonyl. These compounds are useful as an anti-arrhythmic agent.
摘要翻译： 本发明涉及式（I）或（II）的苯并吡喃衍生物或其药学上可接受的盐，其中R1和R2彼此独立地为氢原子，C1-6烷基或C6-14芳基，R3为氢原子或C1- C 1-6烷基羰基氧基或与R 4一起形成键，R 4是氢原子，或与R 3一起形成键，m是0-4的整数，n是0-4的整数，V是单键，CR7R8， NR9，O，S，SO或SO2，R5是氢原子或C1-6烷基，R6是氢原子，C1-6烷基，C3-8环烷基，C3-8环烯基，氨基，C1-6烷基氨基， C 1-6烷基氨基，C 6-14芳基氨基，C 2-9杂芳基氨基，C 6-14芳基，C 2-9杂芳基或C 2-9杂环基，A是与苯环稠合的5-，6-或7-元环作为构成原子 的环，氧原子，氮原子或硫原子可以单独或组合1〜3的数量包含在t中的不饱和键的数量 环是1,2或3，包括待稠合的苯环的不饱和键，构成环的碳原子可以是羰基或硫代羰基。 这些化合物可用作抗心律不齐剂。
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17.发明申请ALPHA-AMINO ACID DERIVATIVES AND MEDICAMENTS CONTAINING THE SAME AS AN ACTIVE INGREDIENT 有权ALPHA-氨基酸衍生物和含有其作为活性成分的药物公开(公告)号：US20090275623A1
公开(公告)日：2009-11-05
申请号：US12306901
申请日：2007-06-29
申请人： Kazuhiko Ohrai , Michiaki Adachi , Koji Toyama , Takanori Shimizu , Keishi Hayashi , Masataka Minami , Yoshiyuki Suzuki , Masakazu Sugiyama , Masateru Ohta , Shojiro Kadono , Takuya Shiraishi , Haruhiko Sato , Yoshiaki Watanabe , Nobuya Ishii , Masahiro Sakaitani , Masami Hasegawa
发明人： Kazuhiko Ohrai , Michiaki Adachi , Koji Toyama , Takanori Shimizu , Keishi Hayashi , Masataka Minami , Yoshiyuki Suzuki , Masakazu Sugiyama , Masateru Ohta , Shojiro Kadono , Takuya Shiraishi , Haruhiko Sato , Yoshiaki Watanabe , Nobuya Ishii , Masahiro Sakaitani , Masami Hasegawa
IPC分类号： A61K31/429 , C07D513/04 , A61P9/04 , A61P35/00
CPC分类号： C07D513/04
摘要： The present invention provides novel α-amino acid derivatives of formula (1): (wherein, R1, R2, R3, R4, X and Y are as defined in the claims) or pharmaceutically acceptable salts, prodrugs or solvates thereof. The derivatives of formula (1) have βARK1 inhibitory activity and are useful for preventing or treating heart failure. Moreover, the derivatives of formula (1) also have antitumor activity, particularly dual inhibitory activity on Aurora kinase and CDK, and are useful for cell proliferative diseases such as cancer.
摘要翻译： 本发明提供新的式（1）的α-氨基酸衍生物：（其中，R 1，R 2，R 3，R 4，X和Y如权利要求中所定义）或其药学上可接受的盐，前药或溶剂合物。 式（1）的衍生物具有βARK1抑制活性，可用于预防或治疗心力衰竭。 此外，式（1）的衍生物还具有抗肿瘤活性，特别是对Aurora激酶和CDK的双重抑制活性，并且可用于细胞增殖性疾病如癌症。
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