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1. 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。

2. 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。

3. 发明授权

US5444084A Substituted heterocyclic derivative having squalene epoxidase inhibition action and its use 失效
标题翻译：具有角鲨烯环氧酶抑制作用的取代杂环衍生物及其用途
公开(公告)号：US5444084A
公开(公告)日：1995-08-22
申请号：US190065
申请日：1994-02-11
申请人： Yoshimi Tsuchiya , Takashi Nomoto , Morihiro Mitsuya , Katsumasa Nonoshita , Masahiro Hayashi , Toshihiko Satoh , Yoshio Sawasaki , Toshio Kamei
发明人： Yoshimi Tsuchiya , Takashi Nomoto , Morihiro Mitsuya , Katsumasa Nonoshita , Masahiro Hayashi , Toshihiko Satoh , Yoshio Sawasaki , Toshio Kamei
IPC分类号： C07D333/08 , C07D333/16 , C07D333/18 , C07D333/24 , A61K31/38
CPC分类号： C07D333/08 , C07D333/16 , C07D333/18 , C07D333/24
摘要： Substituted heterocyclic derivatives represented by the formula (I) ##STR1## wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, Q.sup.1, Q.sup.2, Q.sup.3, Q.sup.4, X and Y are as defined, including, specifically, the compound (E)-3-[3-[3-(2-methoxymethyl-8,8-dimethyl-4-nonen-6-ynyl)phenoxymethyl]phenyl]thiophene, exhibit squalene epoxidase inhibiting activity and are useful in the treatment or prophylaxis of hypercholesterolemia, hyperlipidemia and arteriosclerosis.
摘要翻译： PCT No.PCT / JP93 / 00723 Sec。 371日期1994年2月11日 102（e）日期1994年2月11日PCT提交1993年5月28日PCT公布。出版物WO93 / 24478 （I）表示的取代的杂环衍生物其中R，R1，R2，R3，R4，Q1，Q2，Q3，Q4，X和Y如上所定义，包括具体而言，化合物（E）-3- [3- [3-（2-甲氧基甲基-8,8-二甲基-4-壬烯-6-炔基）苯氧基甲基]苯基]噻吩表现出角鲨烯环氧酶抑制活性，治疗或预防高胆固醇血症，高脂血症和动脉硬化。

4. 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。

5. 发明授权

US6017956A N,N-disubstituted amic acid derivatives 失效
标题翻译： N，N-二取代的酰胺酸衍生物
公开(公告)号：US6017956A
公开(公告)日：2000-01-25
申请号：US47308
申请日：1998-03-25
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： A01N37/00 , A61K31/19 , A61K31/215 , A61K31/505 , C07C233/13 , C07C233/25 , C07C233/47 , C07D213/81 , C07D239/42 , C07D261/18 , C07D271/06 , C07D307/42 , C07D307/68 , C07D405/12 , C07D407/06 , C07D409/14 , C07D417/12
CPC分类号： C07D213/81 , C07C233/13 , C07C233/25 , C07C233/47 , C07D261/18 , C07D271/06 , C07D307/42 , C07D307/68 , C07D405/12 , C07D407/06 , C07D409/14 , C07D417/12
摘要： The present invention relates to a compound of the formula (I): ##STR1## wherein Ar.sup.1, Ar.sup.2, Ar.sup.3 and Ar.sup.4 represent an aryl group or a heteroaromatic ring group; A represents a hydrocarbon group which may be substituted; X and Y represent an oxygen atom, a sulfur atom, a carbonyl group or a group of the formula --CHR.sup.a -- (wherein R.sup.a is a hydrogen atom or a lower alkyl group) or --NR.sup.b -- (wherein R.sup.b is a hydrogen atom or a lower alkyl group), or X and Y together represent a vinylene group or an ethynylene group; R.sup.1, R.sup.2, R.sup.3, R.sup.8 and R.sup.9 represent a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group or a lower alkoxy group; R.sup.4 and R.sup.5 represent a hydrogen atom, a halogen atom, a hydroxyl group, an amino group, a nitro group, a cyano group, a carboxyl group, a lower alkoxycarbonyl group, a carbamoyl group, a lower alkylcarbamoyl group, a lower alkyl group, a lower hydroxyalkyl group, a lower fluoroalkyl group or a lower alkoxy group; R.sup.6 is a lower alkyl group; and R.sup.7 is a hydrogen atom or a lower alkyl group, provided that when one of X and Y is an oxygen atom, a sulfur atom or a group of the formula --NR.sup.b --, the other is a carbonyl group or a group of the formula --CHR.sup.a --, its pharmaceutically acceptable salt or ester, and an antitumor agent containing it as an active ingredient.
摘要翻译：本发明涉及式（I）化合物：其中Ar1，Ar2，Ar3和Ar4表示芳基或杂芳环; A表示可以被取代的烃基; X和Y表示氧原子，硫原子，羰基或式-CHRa-（其中Ra是氢原子或低级烷基）或-NRb-（其中Rb是氢原子或低级烷基），或X和Y一起表示亚乙烯基或亚乙炔基; R1，R2，R3，R8和R9表示氢原子，卤素原子，羟基，低级烷基或低级烷氧基; R4和R5表示氢原子，卤素原子，羟基，氨基，硝基，氰基，羧基，低级烷氧基羰基，氨基甲酰基，低级烷基氨基甲酰基，低级烷基，低级羟烷基，低级氟代烷基或低级烷氧基; R6是低级烷基; 并且R 7是氢原子或低级烷基，条件是当X和Y中的一个是氧原子，硫原子或式-NRb-的基团时，另一个是羰基或式 -CHRa-，其药学上可接受的盐或酯，以及含有它作为活性成分的抗肿瘤剂。

6. 发明授权

US5981573A N,N-disubstituted amic acid derivatives 失效
标题翻译： N，N-二取代的酰胺酸衍生物
公开(公告)号：US5981573A
公开(公告)日：1999-11-09
申请号：US117532
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 , C07D213/56 , C07D307/66 , C07D405/12 , C07D407/12 , C07D307/54 , A61K31/34
CPC分类号： C07D405/12 , C07C233/01 , C07D213/56 , C07D307/66 , C07D407/12
摘要： A compound represented by general formula (I) or a pharmaceutically acceptable salt or ester thereof: [wherein each of Ar.sup.1, Ar.sup.2, Ar.sup.3 and Ar.sup.4 is an aryl group or an aromatic heterocyclic group; A.sup.1 is a C.sub.2-6 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.2-8 chain hydrocarbon group; each of X and Y is an oxygen atom, a sulfur atom, a carbonyl group or a group represented by --CHR.sup.a -- or by --NR.sup.b --, or X and Y together represent a vinylene group or an ethynylene group; each of R.sup.1, R.sup.2, R.sup.3, R.sup.7 and R.sup.8 is a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group, a lower alkenyl group or a lower alkoxy group; each of R.sup.4 and R.sup.5 is a hydrogen atom, a halogen atom, a hydroxyl group, an amino group, a nitro group, a cyano group, a carboxyl group, a lower alkoxycarbonyl group, a carbamoyl group, a lower alkylcarbamoyl group, a lower alkyl group, a lower hydroxyalkyl group, a lower fluoroalkyl group or a lower alkoxy group; and R.sup.6 is a lower alkyl group, provided that when one of X and Y is an oxygen atom, a sulfur atom or a group represented by --NR.sup.b --, the other is a carbonyl group or a group represented by --CHR.sup.a -- and an antitumor agent comprising it as an active ingredient.
摘要翻译： PCT No.PCT / JP97 / 00305 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。出版物WO97 / 29074 日期：1997年8月14日由通式（I）表示的化合物或其药学上可接受的盐或酯：[其中Ar 1，Ar 2，Ar 3和Ar 4各自为芳基或芳族杂环基; A1是C2-6链烃基或由-A1a-W1-A1b-表示的基团（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; A2 是C2-8链烃基; X和Y各自为氧原子，硫原子，羰基或由-CHRa或-NRb-表示的基团，或X和Y一起表示亚乙烯基或一个亚乙炔基; R 1，R 2，R 3，R 7和R 8各自为氢原子，卤素原子，羟基，低级烷基，低级烯基或低级烷氧基; R 4和R 5各自为氢原子，卤素原子，羟基，氨基，硝基，氰基，羧基，低级烷氧基羰基，氨基甲酰基，低级烷基氨基甲酰基，低级烷基，低级羟烷基低级氟烷基或低级烷氧基; R6为低级烷基，条件是当X和Y中的一个为氧原子时，硫原子或基团由-NRb-反射，另一个是由-CHRa表示的羰基或基团，和包含它作为活性成分的抗肿瘤剂。

7. 发明授权

US5643958A Substituted amide derivatives 失效
标题翻译：取代的酰胺衍生物
公开(公告)号：US5643958A
公开(公告)日：1997-07-01
申请号：US616308
申请日：1996-03-15
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： C07C233/05 , C07C233/13 , C07C233/18 , C07C233/25 , C07C233/36 , C07D213/40 , C07D215/12 , C07D235/14 , C07D263/56 , C07D277/64 , C07D307/81 , C07D317/58 , C07D333/58 , C07D413/06 , C07D413/12 , C07D413/14 , A61K31/19 , C07C229/22 , C07C229/24
CPC分类号： C07D213/40 , C07C233/05 , C07C233/13 , C07C233/18 , C07C233/25 , C07C233/36 , C07D215/12 , C07D235/14 , C07D263/56 , C07D277/64 , C07D307/81 , C07D317/58 , C07D333/58 , C07D413/06 , C07D413/12 , C07D413/14
摘要： The present invention relates to a compound of the formula (I): ##STR1## wherein Ar.sup.1, Ar.sup.2 and Ar.sup.3 represent an aryl group or a heteroaromatic ring group; A represents a hydrocarbon group which may be substituted; Q represents a group of the formula --(CH.sub.2).sub.m -- (m is an integer of from 1 to 6) or --(CH.sub.2).sub.n --W--(CH.sub.2).sub.p -- (W is an oxygen atom, a sulfur atom, a vinylene group or an ethynylene group; n and p are a integer of from 0 to 3); R.sup.1 represents a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group, a lower alkoxy group, an aryl or heteroaromatic ring group which may be substituted; R.sup.2, R.sup.7 and R.sup.8 represent a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group or a lower alkoxy group; R.sup.3 and R.sup.4 represent a hydrogen atom, a halogen atom, a hydroxyl group, an amino group, a nitro group, a cyano group, a carboxyl group, a lower alkoxycarbonyl group, a carbamoyl group, a lower alkylcarbamoyl group, a lower alkyl group, a lower hydroxyalkyl group, a lower fluoroalkyl group or a lower alkoxy group; R.sup.5 represents a lower alkyl group; and R.sup.6 represents a hydrogen atom or a lower alkyl group, its pharmaceutically acceptable salt or ester, and an antitumor agent containing it as an active ingredient.
摘要翻译：本发明涉及式（I）的化合物：其中Ar 1，Ar 2和Ar 3表示芳基或杂芳环; A表示可以被取代的烃基; Q表示式 - （CH 2）m - （m为1至6的整数）或 - （CH 2）n W-（CH 2）p - （W为氧原子，硫原子，亚乙烯基）或亚乙炔基; n和p为0〜3的整数）; R1表示氢原子，卤素原子，羟基，低级烷基，低级烷氧基，可被取代的芳基或杂芳族环基; R2，R7和R8表示氢原子，卤素原子，羟基，低级烷基或低级烷氧基; R3和R4表示氢原子，卤素原子，羟基，氨基，硝基，氰基，羧基，低级烷氧基羰基，氨基甲酰基，低级烷基氨基甲酰基，低级烷基，低级羟烷基，低级氟代烷基或低级烷氧基; R5表示低级烷基; R6表示氢原子或低级烷基，其药学上可接受的盐或酯，以及含有它作为有效成分的抗肿瘤剂。

8. 发明授权

US5849747A N, n-disubstituted amic acid derivatives 失效
标题翻译： N，n-二取代的酰胺酸衍生物
公开(公告)号：US5849747A
公开(公告)日：1998-12-15
申请号：US616464
申请日：1996-03-15
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： A01N37/00 , A61K31/19 , A61K31/215 , A61K31/505 , C07C233/13 , C07C233/25 , C07C233/47 , C07D213/81 , C07D239/42 , C07D261/18 , C07D271/06 , C07D307/42 , C07D307/68 , C07D405/12 , C07D407/06 , C07D409/14 , C07D417/12
CPC分类号： C07D213/81 , C07C233/13 , C07C233/25 , C07C233/47 , C07D261/18 , C07D271/06 , C07D307/42 , C07D307/68 , C07D405/12 , C07D407/06 , C07D409/14 , C07D417/12
摘要： The present invention relates to a compound of the formula (I): ##STR1## wherein Ar.sup.1, Ar.sup.2, Ar.sup.3 and Ar.sup.4 represent an aryl group or a heteroaromatic ring group; A represents a hydrocarbon group which may be substituted; X and Y represent an oxygen atom, a sulfur atom, a carbonyl group or a group of the formula --CHR.sup.a -- (wherein R.sup.a is a hydrogen atom or a lower alkyl group) or --NR.sup.b -- (wherein R.sup.b is a hydrogen atom or a lower alkyl group), or X and Y together represent a vinylene group or an ethynylene group; R.sup.1, R.sup.2, R.sup.3, R.sup.8 and R.sup.9 represent a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group or a lower alkoxy group; R.sup.4 and R.sup.5 represent a hydrogen atom, a halogen atom, a hydroxyl group, an amino group, a nitro group, a cyano group, a carboxyl group, a lower alkoxycarbonyl group, a carbamoyl group, a lower alkylcarbamoyl group, a lower alkyl group, a lower hydroxyalkyl group, a lower fluoroalkyl group or a lower alkoxy group; R.sup.6 is a lower alkyl group; and R.sup.7 is a hydrogen atom or a lower alkyl group, provided that when one of X and Y is an oxygen atom, a sulfur atom or a group of the formula --NR.sup.b --, the other is a carbonyl group or a group of the formula --CHR.sup.a --, its pharmaceutically acceptable salt or ester, and an antitumor agent containing it as an active ingredient.
摘要翻译：本发明涉及式（I）的化合物：其中Ar 1，Ar 2，Ar 3和Ar 4表示芳基或杂芳环; A表示可以被取代的烃基; X和Y表示氧原子，硫原子，羰基或式-CHRa-（其中Ra是氢原子或低级烷基）或-NRb-（其中Rb是氢原子或低级烷基），或X和Y一起表示亚乙烯基或亚乙炔基; R1，R2，R3，R8和R9表示氢原子，卤素原子，羟基，低级烷基或低级烷氧基; R4和R5表示氢原子，卤素原子，羟基，氨基，硝基，氰基，羧基，低级烷氧基羰基，氨基甲酰基，低级烷基氨基甲酰基，低级烷基，低级羟烷基，低级氟代烷基或低级烷氧基; R6是低级烷基; 并且R 7是氢原子或低级烷基，条件是当X和Y中的一个是氧原子，硫原子或式-NRb-的基团时，另一个是羰基或式 -CHRa-，其药学上可接受的盐或酯，以及含有它作为活性成分的抗肿瘤剂。

9. 发明授权

US6011174A Cyclic amic acid derivatives 失效
标题翻译：环状酰胺酸衍生物
公开(公告)号：US6011174A
公开(公告)日：2000-01-04
申请号：US117534
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： C07C233/51 , C07D317/32 , C07C229/00 , A61K31/195 , A61K31/335 , C07D317/00
CPC分类号： C07C233/51 , C07D317/32
摘要： The present invention relates to a compound of the formula (I), or its pharmaceutically acceptable salt or ester: ##STR1## wherein Ar.sup.1 is an aryl group or a heteroaromatic ring group; Ar is a group of the formula ##STR2## each of Ar.sup.2 and Ar.sup.3 is an aryl group or a heteroaromatic ring group; Cy is an aryl group, a heteroaromatic ring group or an aliphatic ring group which may contain one or two oxygen atoms; A.sup.1 is a C.sub.1-4 chain hydrocarbon group; m is an integer of from 1 to 6; each of n and p is an integer of from 0 to 3; Q.sup.1 is a single bond, a group of the formula --CH.sub.2 O--, --OCH.sub.2 --, --CH.sub.2 S-- or --SCH.sub.2 --, or a C.sub.1-6 chain hydrocarbon group; Q.sup.2 is a single bond or a group of the formula --(CH.sub.2).sub.m -- or --(CH.sub.2).sub.n --W--(CH.sub.2).sub.p --; Q.sup.3 is a single bond, an oxygen atom, a sulfur atom, a methylene group, a vinylene group or a group of the formula --CO--, --NH--, --COO--, --OCO--, --CH.sub.2 CH.sub.2 --, --OCH.sub.2 --, --SCH.sub.2 --, --CH.sub.2 O--, --CH.sub.2 S--, --NHCO-- or --CONH--; R.sup.1 is a lower alkyl group; each of R.sup.2 and R.sup.3 is a hydrogen atom, a hydroxyl group or a lower alkyl group; W is an oxygen atom, a sulfur atom, a vinylene group or an ethynylene group; x is an integer of from 0 to 2; and y is 0 or 1; and an antitumor agent containing it as an active ingredient and intermediates for the production thereof.
摘要翻译： PCT No.PCT / JP97 / 00303 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。出版物WO97 / 29078 日期：1997年8月14日本发明涉及式（I）化合物或其药学上可接受的盐或酯：其中Ar1为芳基或杂芳环; Ar是下式的基团：Ar 2和Ar 3是芳基或杂芳环; Cy是可以含有一个或两个氧原子的芳基，杂芳族环基团或脂族环基团; A1是C1-4链烃基; m为1〜6的整数; n和p各自为0至3的整数; Q1是单键，式-CH 2 O - ， - OCH 2 - ， - CH 2 S-或-SCH 2 - 或C 1-6链烃基的基团; Q 2是单键或式 - （CH 2）m - 或 - （CH 2）n -W-（CH 2）p - 的基团; Q3是单键，氧原子，硫原子，亚甲基，亚乙烯基或式-CO-，-NH-，-COO-，-OCO-， - CH 2 CH 2 - ， - OCH 2 - ，-SCH 2 - ， - CH 2 O - ， - CH 2 S - ， - NHCO-或-CONH-; R1是低级烷基; R2和R3各自为氢原子，羟基或低级烷基; W是氧原子，硫原子，亚乙烯基或亚乙炔基; x是0至2的整数; y为0或1; 和含有它作为活性成分的抗肿瘤剂和用于制备它的中间体。

10. 发明授权

US5919786A N,N-disubstituted amic acid derivatives 失效
标题翻译： N，N-二取代的酰胺酸衍生物
公开(公告)号：US5919786A
公开(公告)日：1999-07-06
申请号：US47311
申请日：1998-03-25
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： A01N37/00 , A61K31/19 , A61K31/215 , A61K31/505 , C07C233/13 , C07C233/25 , C07C233/47 , C07D213/81 , C07D239/42 , C07D261/18 , C07D271/06 , C07D307/42 , C07D307/68 , C07D405/12 , C07D407/06 , C07D409/14 , C07D417/12 , A61K31/44 , C07D213/02 , C07D239/26
CPC分类号： C07D213/81 , C07C233/13 , C07C233/25 , C07C233/47 , C07D261/18 , C07D271/06 , C07D307/42 , C07D307/68 , C07D405/12 , C07D407/06 , C07D409/14 , C07D417/12
摘要： The present invention relates to a compound of the formula (I): ##STR1## wherein Ar.sup.1, Ar.sup.2, Ar.sup.3 and Ar.sup.4 represent an aryl group or a heteroaromatic ring group; A represents a hydrocarbon group which may be substituted; X and Y represent an oxygen atom, a sulfur atom, a carbonyl group or a group of the formula --CHR.sup.a -- (wherein R.sup.a is a hydrogen atom or a lower alkyl group) or --NR.sup.b -- (wherein R.sup.b is a hydrogen atom or a lower alkyl group), or X and Y together represent a vinylene group or an ethynylene group; R.sup.1, R.sup.2, R.sup.3, R.sup.8 and R.sup.9 represent a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group or a lower alkoxy group; R.sup.4 and R.sup.5 represent a hydrogen atom, a halogen atom, a hydroxyl group, an amino group, a nitro group, a cyano group, a carboxyl group, a lower alkoxycarbonyl group, a carbamoyl group, a lower alkylcarbamoyl group, a lower alkyl group, a lower hydroxyalkyl group, a lower fluoroalkyl group or a lower alkoxy group, R.sup.6 is a lower alkyl group, and R.sup.7 is a hydrogen atom or a lower alkyl group, provided that when one of X and Y is an oxygen atom, a sulfur atom or a group of the formula --NR.sup.b --, the other is a carbonyl group or a group of the formula --CHR.sup.a --, its pharmaceutically acceptable salt or ester, and an antitumor agent containing it as an active ingredient.
摘要翻译：本发明涉及式（I）化合物：其中Ar1，Ar2，Ar3和Ar4表示芳基或杂芳环; A表示可以被取代的烃基; X和Y表示氧原子，硫原子，羰基或式-CHRa-（其中Ra是氢原子或低级烷基）或-NRb-（其中Rb是氢原子或低级烷基），或X和Y一起表示亚乙烯基或亚乙炔基; R1，R2，R3，R8和R9表示氢原子，卤素原子，羟基，低级烷基或低级烷氧基; R4和R5表示氢原子，卤素原子，羟基，氨基，硝基，氰基，羧基，低级烷氧基羰基，氨基甲酰基，低级烷基氨基甲酰基，低级烷基低级羟烷基，低级氟烷基或低级烷氧基，R6为低级烷基，R7为氢原子或低级烷基，条件是当X和Y中的一个为氧原子时，硫原子或式-NRb-的基团，另一个是羰基或式-CHRa-基团，其药学上可接受的盐或酯，以及含有它作为活性成分的抗肿瘤剂。

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