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1. 发明授权

US5405873A Substituted acetamide derivatives 失效
标题翻译：取代的乙酰胺衍生物
公开(公告)号：US5405873A
公开(公告)日：1995-04-11
申请号：US117891
申请日：1993-09-07
申请人： Yoshikazu Iwasawa , Hiromi Hattori , Yasufumi Nagata , Akiko Shimizu , Yoshio Sawasaki
发明人： Yoshikazu Iwasawa , Hiromi Hattori , Yasufumi Nagata , Akiko Shimizu , Yoshio Sawasaki
IPC分类号： C07C317/44 , C07C323/60 , C07D215/36 , C07D233/28 , C07D233/84 , C07D239/38 , C07D307/91 , C07D333/18 , A61K31/165 , C07C321/24 , C07C323/23
CPC分类号： C07D307/91 , C07C317/44 , C07C323/60 , C07D215/36 , C07D233/28 , C07D239/38 , C07D333/18 , Y10S514/824
摘要： There are provided substituted acetamide derivatives represented by general formula (I): ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.10, R.sup.11, R.sup.12, R.sup.13, n and Z are defined in the specification. The substituted acetamide derivatives strongly inhibit acylcoenzyme A cholesterol acyltransferase (ACTA) and are expected to be effective for the treatment and prevention of hypercholesterolemia, hyperlipemia and arteriosclerosis.
摘要翻译：提供由通式（I）表示的取代的乙酰胺衍生物：其中R1，R2，R3，R4，R5，R6，R7，R8，R9，R10，R11，R12，R13，n和Z 在规范中定义。取代的乙酰胺衍生物强烈地抑制酰基辅酶A胆固醇酰基转移酶（ACTA），并且预期对于治疗和预防高胆固醇血症，高脂血症和动脉硬化是有效的。

2. 发明授权

US5616803A Substituted amic acid derivatives 失效
标题翻译：取代的酰胺酸衍生物
公开(公告)号：US5616803A
公开(公告)日：1997-04-01
申请号：US540628
申请日：1995-10-06
申请人： Takashi Nomoto , Masahiro Hayashi , Jun Shibata , Yoshikazu Iwasawa , Morihiro Mitsuya , Yoshiaki Iida , Katsumasa Nonoshita , Yasufumi Nagata
发明人： Takashi Nomoto , Masahiro Hayashi , Jun Shibata , Yoshikazu Iwasawa , Morihiro Mitsuya , Yoshiaki Iida , Katsumasa Nonoshita , Yasufumi Nagata
IPC分类号： C07C69/34 , C07C211/27 , C07C211/29 , C07C215/52 , C07C217/60 , C07C233/05 , C07C233/13 , C07C233/18 , C07C235/06 , C07D213/38 , C07D213/40 , C07D215/12 , C07D215/48 , C07D263/32 , C07D307/14 , C07D307/52 , C07D307/81 , C07D317/58 , C07D333/20 , C07D333/28 , C07D333/54 , C07D333/58
CPC分类号： C07D213/40 , C07C211/27 , C07C211/29 , C07C215/52 , C07C217/60 , C07C233/05 , C07C233/13 , C07C233/18 , C07C235/06 , C07C69/34 , C07D213/38 , C07D215/12 , C07D215/48 , C07D263/32 , C07D307/14 , C07D307/52 , C07D307/81 , C07D317/58 , C07D333/20 , C07D333/28 , C07D333/54 , C07D333/58
摘要： A compound of the formula (I) or its pharmaceutically acceptable salt or ester: ##STR1## wherein each of the substituents are herein defined.
摘要翻译：式（I）化合物或其药学上可接受的盐或酯：其中每个取代基在本文中定义。

3. 发明授权

US5606101A Substitute amic acid derivatives 失效
标题翻译：取代酰胺酸衍生物
公开(公告)号：US5606101A
公开(公告)日：1997-02-25
申请号：US540329
申请日：1995-10-06
申请人： Takashi Nomoto , Masahiro Hayashi , Jun Shibata , Yoshikazu Iwasawa , Morihiro Mitsuya , Yoshiaki IIda , Katsumasa Nonoshita , Yasufumi Nagata
发明人： Takashi Nomoto , Masahiro Hayashi , Jun Shibata , Yoshikazu Iwasawa , Morihiro Mitsuya , Yoshiaki IIda , Katsumasa Nonoshita , Yasufumi Nagata
IPC分类号： C07C69/34 , C07C211/27 , C07C211/29 , C07C215/52 , C07C217/60 , C07C233/05 , C07C233/13 , C07C233/18 , C07C235/06 , C07D213/38 , C07D213/40 , C07D215/12 , C07D215/48 , C07D263/32 , C07D307/14 , C07D307/52 , C07D307/81 , C07D317/58 , C07D333/20 , C07D333/28 , C07D333/54 , C07D333/58 , C07C69/353
CPC分类号： C07D213/40 , C07C211/27 , C07C211/29 , C07C215/52 , C07C217/60 , C07C233/05 , C07C233/13 , C07C233/18 , C07C235/06 , C07C69/34 , C07D213/38 , C07D215/12 , C07D215/48 , C07D263/32 , C07D307/14 , C07D307/52 , C07D307/81 , C07D317/58 , C07D333/20 , C07D333/28 , C07D333/54 , C07D333/58
摘要： A compound of the formula (I) or its pharmaceutically acceptable salt or ester: ##STR1## and intermediates thereof.
摘要翻译：式（I）化合物或其药学上可接受的盐或酯：其中和（I）及其中间体。

4. 发明授权

US5488149A Substituted amic acid derivatives 失效
标题翻译：取代的酰胺酸衍生物
公开(公告)号：US5488149A
公开(公告)日：1996-01-30
申请号：US471081
申请日：1995-06-06
申请人： Takashi Nomoto , Masahiro Hayashi , Jun Shibata , Yoshikazu Iwasawa , Morihiro Mitsuya , Yoshiaki Iida , Katsumasa Nonoshita , Yasufumi Nagata
发明人： Takashi Nomoto , Masahiro Hayashi , Jun Shibata , Yoshikazu Iwasawa , Morihiro Mitsuya , Yoshiaki Iida , Katsumasa Nonoshita , Yasufumi Nagata
IPC分类号： C07C69/34 , C07C211/27 , C07C211/29 , C07C215/52 , C07C217/60 , C07C233/05 , C07C233/13 , C07C233/18 , C07C235/06 , C07D213/38 , C07D213/40 , C07D215/12 , C07D215/48 , C07D263/32 , C07D307/14 , C07D307/52 , C07D307/81 , C07D317/58 , C07D333/20 , C07D333/28 , C07D333/54 , C07D333/58 , C07C235/72
CPC分类号： C07D213/40 , C07C211/27 , C07C211/29 , C07C215/52 , C07C217/60 , C07C233/05 , C07C233/13 , C07C233/18 , C07C235/06 , C07C69/34 , C07D213/38 , C07D215/12 , C07D215/48 , C07D263/32 , C07D307/14 , C07D307/52 , C07D307/81 , C07D317/58 , C07D333/20 , C07D333/28 , C07D333/54 , C07D333/58
摘要： A compound of the formula (I) or its pharmaceutically acceptable salt or ester: ##STR1## wherein each of the substituents are herein defined.
摘要翻译：式（I）化合物或其药学上可接受的盐或酯：其中每个取代基在本文中定义。

5. 发明授权

US5777150A Substituted amic acid derivatives 失效
标题翻译：取代的酰胺酸衍生物
公开(公告)号：US5777150A
公开(公告)日：1998-07-07
申请号：US696152
申请日：1996-08-13
申请人： Takashi Nomoto , Masahiro Hayashi , Jun Shibata , Yoshikazu Iwasawa , Morihiro Mitsuya , Yoshiaki Iida , Katsumasa Nonoshita , Yasufumi Nagata
发明人： Takashi Nomoto , Masahiro Hayashi , Jun Shibata , Yoshikazu Iwasawa , Morihiro Mitsuya , Yoshiaki Iida , Katsumasa Nonoshita , Yasufumi Nagata
IPC分类号： C07C69/34 , C07C211/27 , C07C211/29 , C07C215/52 , C07C217/60 , C07C233/05 , C07C233/13 , C07C233/18 , C07C235/06 , C07D213/38 , C07D213/40 , C07D215/12 , C07D215/48 , C07D263/32 , C07D307/14 , C07D307/52 , C07D307/81 , C07D317/58 , C07D333/20 , C07D333/28 , C07D333/54 , C07D333/58 , C07C69/78 , C07C69/767 , C07C69/773 , C07D317/34
CPC分类号： C07D213/40 , C07C211/27 , C07C211/29 , C07C215/52 , C07C217/60 , C07C233/05 , C07C233/13 , C07C233/18 , C07C235/06 , C07C69/34 , C07D213/38 , C07D215/12 , C07D215/48 , C07D263/32 , C07D307/14 , C07D307/52 , C07D307/81 , C07D317/58 , C07D333/20 , C07D333/28 , C07D333/54 , C07D333/58
摘要： A compound of the formula (I) or its pharmaceutically acceptable salt or ester: ##STR1## wherein each of ##STR2## which are the same or different, is an aryl group or a heteroaromatic ring group; A is a C.sub.3-8 linear saturated or unsaturated aliphatic hydrocarbon group which may have substituent(s) selected from the group consisting of a lower alkyl group, a hydroxyl group, a lower alkoxy group, a carboxyl group, an aryl group and an aralkyl group; Q is a single bond or a group of the formula --CO--O--, --O--CO--, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, --OCH.sub.2 --, --SCH.sub.2 --, --CH.sub.2 O-- or --CH.sub.2 S--; each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 which are the same or different, is a hydrogen atom, a halogen atom, a lower alkyl group, a hydroxyl group, a lower alkoxy group, or an aryl or heteroaromatic ring group which may have substituent(s) selected from the group consisting of a halogen atom, a lower alkyl group and a lower alkoxy group; each of R.sup.5, R.sup.6 and R.sup.7 which are the same or different, is a hydrogen atom or a lower alkyl group; and R.sup.8 is a hydrogen atom, a lower alkyl group, a lower alkenyl group, a lower alkynyl group or an aralkyl group, provided that when Q is a single bond, ##STR3## are not simultaneously 4-chlorophenyl groups.
摘要翻译：式（I）化合物或其药学上可接受的盐或酯：其中每个相同或不同的芳基是芳基或杂芳环; A是可以具有选自低级烷基，羟基，低级烷氧基，羧基，芳基和芳烷基的取代基的C3-8直链饱和或不饱和脂族烃基组; Q是单键或式-CO-O-，-O-CO-，-CH 2 CH 2 - ， - CH = CH - ， - OCH 2 - ， - CH 2 - ， - CH 2 O-或-CH 2 S--的基团; R 1，R 2，R 3和R 4相同或不同的是氢原子，卤素原子，低级烷基，羟基，低级烷氧基或可具有取代基的芳基或杂芳族环基选自卤素原子，低级烷基和低级烷氧基的基团; R 5，R 6和R 7各自相同或不同，为氢原子或低级烷基; 并且R8是氢原子，低级烷基，低级烯基，低级炔基或芳烷基，条件是当Q为单键时，＆lt; IMAGE＆gt;不同时为4-氯苯基。

6. 发明授权

US5439932A Substituted amine derivatives having anti-hyperlipemia activity 失效
标题翻译：具有抗高血脂活性的取代的胺衍生物
公开(公告)号：US5439932A
公开(公告)日：1995-08-08
申请号：US26692
申请日：1993-03-04
申请人： Yoshimi Tsuchiya , Takashi Nomoto , Masahiro Hayashi , Yoshikazu Iwasawa , Hitoshi Masaki , Mitsuru Ohkubo , Yumiko Sakuma , Yasufumi Nagata , Toshihiko Satoh , Toshio Kamei
发明人： Yoshimi Tsuchiya , Takashi Nomoto , Masahiro Hayashi , Yoshikazu Iwasawa , Hitoshi Masaki , Mitsuru Ohkubo , Yumiko Sakuma , Yasufumi Nagata , Toshihiko Satoh , Toshio Kamei
IPC分类号： C07D213/30 , C07D263/32 , C07D277/24 , C07D333/16 , C07D333/18 , C07D333/20 , C07D333/24 , C07D333/32 , C07D409/12 , C07D413/12 , C07D417/12 , C07D521/00 , A61K31/38 , A61K31/495 , C07D409/02 , C07D409/14
CPC分类号： C07D213/30 , C07D231/12 , C07D233/56 , C07D249/08 , C07D263/32 , C07D277/24 , C07D333/16 , C07D333/18 , C07D333/20 , C07D333/24 , C07D333/32 , C07D409/12 , C07D413/10 , C07D417/12
摘要： Substituted amine derivatives represented by the general formula ##STR1## wherein Q is --C--D--E--F--G--M-- or --N--H--I--J--K--L-- [C, D, E, F, G, H, I, J, K and L are each O, S, a carbonyl group, --CHR.sup.a --, --R.sup.b .dbd. or --NR.sup.c -- (R.sup.a, R.sup.b and R.sup.c are each H or a lower alkyl group), M and N are each an aromatic ring of 5-6 members optionally having a halogen, OH, LN, a lower alkyl group or a lower alkoxy group, provided that L is not O, S, or --NR.sup.c --]; R is a heterocyclic ring of 5-6 members; R.sup.1 is H, a lower alkyl group, a lower haloalkyl group, a lower alkenyl group, a lower alkynyl group or a cycloalkyl group; R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 are each H, a halogen or a lower alkyl group or two of them denote a single bond; R.sup.8 and R.sup.9 are each F, CF.sub.3 or a lower alkyl group or are a cycloalkane in combination thereof; and R.sup.10 is H, F, CF.sub.3 an acetoxy group, a lower alkyl group or a lower alkoxy group. These compounds inhibit biosynthesis of cholesterol in mammals by inhibiting their squalene epoxidase, and thereby lower their blood cholesterol values. Therefore, these compounds are expected to be effective as an agent for treatment and prophylaxis of diseases caused by excess of cholesterol, for example, obesity, hyperlipemia and arteriosclerosis and heart and encephalic diseases accompanying them.
摘要翻译：由通式[IMAGE] [I]表示的取代的胺衍生物，其中Q是-_ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ ，_F，_G，_H，_I，_J，_K和_L各自为O，S，羰基，-CHR a - ，-R b =或-NR c - （R a，R b和R c各自为H或低级烷基） M和N各自为任选具有卤素，OH，LN，低级烷基或低级烷氧基的5-6个成员的芳环，条件是_L不是O，S或-NRc-]; R是5-6个成员的杂环; R1是H，低级烷基，低级卤代烷基，低级烯基，低级炔基或环烷基; R2，R3，R4，R5，R6和R7各自为H，卤素或低级烷基，或两个表示单键; R8和R9各自为F，CF3或低级烷基，或其组合为环烷烃; R 10为H，F，CF 3为乙酰氧基，低级烷基或低级烷氧基。这些化合物通过抑制它们的角鲨烯环氧酶抑制哺乳动物胆固醇的生物合成，从而降低它们的血液中胆固醇值。因此，预期这些化合物作为用于治疗和预防由胆固醇过量引起的疾病，例如肥胖症，高脂血症和动脉硬化以及与其伴随的心脏和脑病有关的药剂。

7. 发明授权

US5306728A Substituted amine derivatives having antihyperlipemia activity 失效
标题翻译：具有抗高血脂活性的取代的胺衍生物
公开(公告)号：US5306728A
公开(公告)日：1994-04-26
申请号：US26120
申请日：1993-03-04
申请人： Yoshimi Tsuchiya , Takashi Nomoto , Masahiro Hayashi , Yoshikazu Iwasawa , Hitoshi Masaki , Mitsuru Ohkubo , Yumiko Sakuma , Yasufumi Nagata , Toshihiko Satoh , Toshio Kamei
发明人： Yoshimi Tsuchiya , Takashi Nomoto , Masahiro Hayashi , Yoshikazu Iwasawa , Hitoshi Masaki , Mitsuru Ohkubo , Yumiko Sakuma , Yasufumi Nagata , Toshihiko Satoh , Toshio Kamei
IPC分类号： C07D213/30 , C07D263/32 , C07D277/24 , C07D333/16 , C07D333/18 , C07D333/20 , C07D333/24 , C07D333/32 , C07D409/12 , C07D413/12 , C07D417/12 , C07D521/00 , A61K31/38 , A01N43/06 , C07D333/10 , C07D411/10
CPC分类号： C07D213/30 , C07D231/12 , C07D233/56 , C07D249/08 , C07D263/32 , C07D277/24 , C07D333/16 , C07D333/18 , C07D333/20 , C07D333/24 , C07D333/32 , C07D409/12 , C07D413/10 , C07D417/12
摘要： Substituted amine derivatives represented by the general formula ##STR1## wherein Q is -C-D-E- F-G-M- or -N-H-I-J-K-L- [C, D, E, F, G, H, I, J, K and L are each O, S, a carbonyl group, -CHR.sup.2 -, -R.sup.b = or -NR.sup.c - (R.sup.a, R.sup.b and R.sup.c are each H or a lower alkyl group), M and N are each an aromatic ring of 5-6 members optionally having a halogen, OH, LN, a lower alkyl group or a lower alkoxy group, provided that L is not O, S, or -NR.sup.c -]; R is a heterocyclic ring of 5-6 members; R.sup.1 is H, a lower alkyl group, a lower haloalkyl group, a lower alkenyl group, a lower alkynyl group or a cycloalkyl group; R.sup.2, R.sup.3, R.sup.4, R.sup.5 R.sup.6 and R.sup.7 are each H, a halogen or a lower alkyl group or two of them denote a single bond; R.sup.8 and R.sup.9 are each F, CF.sub.3 or a lower alkyl group or are a cycloalkane in combination thereof; and R.sup.10 is H, F, CF.sub. 3 an acetoxy group, a lower alkyl group or a lower alkoxy group. These compounds inhibit biosynthesis of cholesterol in mammals by inhibiting their squalene epoxidase, and thereby lower their blood cholesterol values. Therefore, these compounds are expected to be effective as an agent for treatment and prophylaxis of diseases caused by excess of cholesterol, for example, obesity, hyperlipemia and arteriosclerosis and heart and encephalic diseases accompanying them.
摘要翻译：其中Q为-CDE-FGM-或-NHIJKL- [C，D，E，F，G，H，I，J，K和L各自为O， S，羰基，-CHR 2 - ，-R b =或-NR c - （R a，R b和R c各自为H或低级烷基），M和N各自为任选具有卤素的5-6个成员的芳香环，OH，LN，低级烷基或低级烷氧基，条件是L不是O，S或-NRc-]; R是5-6个成员的杂环; R1是H，低级烷基，低级卤代烷基，低级烯基，低级炔基或环烷基; R2，R3，R4，R5 R6和R7各自为H，卤素或低级烷基，或两个表示单键; R8和R9各自为F，CF3或低级烷基，或其组合为环烷烃; R 10为H，F，CF 3为乙酰氧基，低级烷基或低级烷氧基。这些化合物通过抑制它们的角鲨烯环氧酶抑制哺乳动物胆固醇的生物合成，从而降低它们的血液中胆固醇值。因此，预期这些化合物作为用于治疗和预防由胆固醇过量引起的疾病，例如肥胖症，高脂血症和动脉硬化以及与其伴随的心脏和脑病有关的药剂。

8. 发明授权

US07915263B2 Aminopyridine derivatives having aurora A selective inhibitory action 有权
标题翻译：具有极光A的选择性抑制作用的氨基吡啶衍生物
公开(公告)号：US07915263B2
公开(公告)日：2011-03-29
申请号：US11897272
申请日：2007-08-29
申请人： Yoshikazu Iwasawa , Tetsuya Kato , Nobuhiko Kawanishi , Kouta Masutani , Takashi Mita , Katsumasa Nonoshita , Mitsuru Ohkubo
发明人： Yoshikazu Iwasawa , Tetsuya Kato , Nobuhiko Kawanishi , Kouta Masutani , Takashi Mita , Katsumasa Nonoshita , Mitsuru Ohkubo
IPC分类号： C07D401/12 , A61K31/4439
CPC分类号： C07D413/14 , A61K45/06 , C07D401/12 , C07D403/12 , C07D417/12
摘要： The present invention relates to a compound of formula I: wherein: R1 is a hydrogen atom, F, CN, etc.; R1′ is a hydrogen atom or lower alkyl which may be substituted; R2 is O, S, SO, SO2, etc.; R3 is a phenyl which may be substituted; X1, X2, and X3 each independently CH, N, etc. provided, however, that among X1, X2 and X3, the number of nitrogen is 0 or 1; W is the following residue: wherein: W1, W2, and W3 each independently CH, N, etc., or a pharmaceutically acceptable salt or ester thereof.
摘要翻译：本发明涉及式I化合物：其中：R1是氢原子，F，CN等; R1'是氢原子或可被取代的低级烷基; R2是O，S，SO，SO2等; R3是可被取代的苯基; X1，X2和X3各自独立地为CH，N等，但X1，X2和X3之间的氮数为0或1。 W是以下残基：其中：W1，W2和W3各自独立地为CH，N等，或其药学上可接受的盐或酯。

9. 发明申请

US20080081811A1 Selective Inhibitors Against Cdk4 and Cdk6 Having Aminothiazole Skeleton 失效
标题翻译：对具有氨基噻唑骨架的Cdk4和Cdk6的选择性抑制剂
公开(公告)号：US20080081811A1
公开(公告)日：2008-04-03
申请号：US11596735
申请日：2005-05-19
申请人： Yoshikazu Iwasawa , Jun Shibata , Tadashi Shimamura , Hideki Kurihara , Takashi Mita , Nobuhiko Kawanishi , Takashi Hashihayata , Mikako Kawamura , Takeshi Sagara , Sachie Arai , Hiroshi Hirai
发明人： Yoshikazu Iwasawa , Jun Shibata , Tadashi Shimamura , Hideki Kurihara , Takashi Mita , Nobuhiko Kawanishi , Takashi Hashihayata , Mikako Kawamura , Takeshi Sagara , Sachie Arai , Hiroshi Hirai
IPC分类号： A61K31/496 , A61K31/497 , A61K31/505 , A61K31/5377 , A61P35/00 , C07D239/32 , C07D403/14 , C07D413/14
CPC分类号： C07D417/14 , C07D417/12 , C07D491/08
摘要： The present invention relates to a compound represented by Formula [I]: wherein X is O, S, NH or CH2; Y1, Y2, Y3, Y4 and Y5, which may be identical or different, are each CH or N; however, at least one of Y1, Y2, Y3, Y4 and Y5 is N; Z1 and Z2, which may be identical or different, are each CH or N; n is an integer from 1 to 3; R1 is a C3-C8 cycloalkyl group, a C6-C10 aryl group, an aliphatic heterocyclic ring or an aromatic heterocyclic ring, or a bicyclic aliphatic saturated hydrocarbon group; R2 and R3, which may be identical or different, are each a hydrogen atom, a lower alkyl group, a lower alkenyl group, a C3-C8 cycloalkyl group, a C6-C10 aryl group, an aromatic heterocyclic ring, or the like; and R4 is a hydrogen atom, a lower alkyl group, a C3-C6 cycloalkyl group or the like, or a pharmaceutically acceptable salt or ester thereof, and a selective inhibitor against Cdk4 and/or Cdk6 or an anticancer agent containing the compound or a pharmaceutically acceptable salt or ester thereof.
摘要翻译：本发明涉及由式[I]表示的化合物：其中X是O，S，NH或CH 2; Y 1，Y 2，Y 3，Y 4和Y 5，其可以相同或不同，各自为CH或N; 然而，Y 1，Y 2，Y 3，Y 4和Y 3中的至少一个， 5 是N; Z 1和Z 2可以相同或不同，各自为CH或N; n为1〜3的整数， R 1是C 3 -C 8环烷基，C 6 -C 10环烷基，C 6 -C 15环烷基，芳基，脂族杂环或芳族杂环，或双环脂族饱和烃基; R 2和R 3可以相同或不同，分别为氢原子，低级烷基，低级烯基，C 3， C 1 -C 8环烷基，C 6 -C 10芳基，芳族杂环等; 和R 4是氢原子，低级烷基，C 3 -C 6环烷基等，或药学上可接受的盐或酯，以及对Cdk4和/或Cdk6的选择性抑制剂或含有该化合物或其药学上可接受的盐或酯的抗癌剂。

10. 发明授权

US6048894A Substituted amide derivatives 失效
标题翻译：取代的酰胺衍生物
公开(公告)号：US6048894A
公开(公告)日：2000-04-11
申请号：US117533
申请日：1998-08-04
申请人： Yoshikazu Iwasawa , Tetsuya Aoyama , Kumiko Kawakami , Sachie Arai , Toshihiko Satoh , Yoshiaki Monden
发明人： Yoshikazu Iwasawa , Tetsuya Aoyama , Kumiko Kawakami , Sachie Arai , Toshihiko Satoh , Yoshiaki Monden
IPC分类号： C07C233/01 , C07D307/68 , A61K31/34
CPC分类号： C07C233/01 , C07D307/68
摘要： The present invention relates to a compound represented by general formula (I) or a pharmaceutically acceptable salt or ester thereof: ##STR1## [wherein each of ##STR2## is an aryl group or an aromatic heterocyclic group; A.sup.1 is a C.sub.1-6 chain hydrocarbon group or a group represented by --A.sup.1a --W.sup.1 --A.sup.1b -- (wherein W.sup.1 is an oxygen atom, a sulfur atom, an ethynylene group, a cyclopropylene group or a group represented by --NR.sup.W --); A.sup.2 is a C.sub.1-8 chain hydrocarbon group; R.sup.1 is a lower alkyl group, a lower alkenyl group, a lower alkoxy group, a carboxyl group, a lower alkoxycarbonyl group, a carbamoyl group, a lower alkylcarbamoyl group, a group represented by R.sup.a COO-- (wherein R.sup.a is a hydrogen atom, an amino group, a lower alkyl group, a lower alkoxy group or a lower alkylamino group) or by R.sup.b CONR.sup.c -- (wherein R.sup.b is a hydrogen atom, an amino group, a lower alkyl group, a lower alkoxy group or a lower alkylamino group) or an alicyclic group; R.sup.2 is a lower alkyl group; and each of X and Y is an oxygen atom, a sulfur atom, a carbonyl group, a group represented by --CHR.sup.d -- or by --NR.sup.e --, or X and Y together represent a vinylene group or an ethynylene group, provided that when one of X and Y is an oxygen atom, a sulfur atom or group represented by --NR.sup.e --, the other is a carbonyl group or a group represented by --CHR.sup.d --] and an antitumor agent comprising it as an active ingredient.
摘要翻译： PCT No.PCT / JP97 / 00304 Sec。 371日期：1998年8月4日 102（e）日期1998年8月4日PCT提交1997年2月7日PCT公布。公开号WO97 / 29073 日期：1997年8月14日本发明涉及由通式（I）表示的化合物或其药学上可接受的盐或酯：[其中每一个为芳基或芳族杂环基; A1是C1-6链烃基或由-A1a-W1-A1b-（其中W1是氧原子，硫原子，亚乙炔基，亚环丙基或由-NRW-表示的基团）表示的基团; A2是C1-8链烃基; R1是低级烷基，低级烯基，低级烷氧基，羧基，低级烷氧基羰基，氨基甲酰基，低级烷基氨基甲酰基，由RaCOO-表示的基团（其中，Ra是氢原子，氨基，低级烷基，低级烷氧基或低级烷基氨基）或RbCONRc-（其中Rb是氢原子，氨基，低级烷基，低级烷氧基或低级烷基氨基）或脂环族; R2是低级烷基; 并且X和Y各自为氧原子，硫原子，羰基，-CHRd-或-NRe-表示的基团，或X和Y一起表示亚乙烯基或亚乙炔基，条件是当一个的X和Y是氧原子，由-NRe-表示的硫原子或基团，另一个是由-CHRd-]表示的羰基或基团，以及包含其作为活性成分的抗肿瘤剂。

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