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1. 发明授权

US08618312B2 Method of producing bicyclo[3.1.0] hexane derivative using enzyme 失效
标题翻译：使用酶制备双环[3.1.0]己烷衍生物的方法
公开(公告)号：US08618312B2
公开(公告)日：2013-12-31
申请号：US12950609
申请日：2010-11-19
申请人： Mitsuaki Hirotsuka , Joji Sasaki , Hiroaki Kamiyama , Motoko Oshida , Takaaki Ishii
发明人： Mitsuaki Hirotsuka , Joji Sasaki , Hiroaki Kamiyama , Motoko Oshida , Takaaki Ishii
IPC分类号： C07D327/04 , C07D317/72
CPC分类号： C12P7/62 , C07C67/31 , C07C67/313 , C07C67/32 , C07C67/327 , C07C67/343 , C07C2602/18 , C07D317/72 , C07C69/757 , C07C69/732
摘要： Production of a bicyclo[3.1.0]hexane derivative, useful as a metabotropic glutamate receptor modulator, becomes possible by a production method that includes converting a compound represented by Formula (II) into a compound represented by Formula (III) by reaction with an acyl group donor in the presence of a microorganism-derived enzyme, without using an expensive optically active trans hydroxy ester as a starting material and without employing a fluorination reaction requiring an ultralow temperature reaction. Furthermore, since asymmetric synthesis can be carried out in a stage closer to the final product, the production method is useful as a production method that can mass produce a bicyclo[3.1.0]hexane derivative.
摘要翻译：作为代谢型谷氨酸受体调节剂有用的双环[3.1.0]己烷衍生物的制备可以通过以下制备方法来实现：包括将由式（II）表示的化合物转化成由式（III）表示的化合物与在不使用昂贵的光学活性羟基羟基酯作为起始原料的情况下，在微生物衍生的酶的存在下，不需要超低温反应的氟化反应。此外，由于不对称合成可以在更接近最终产物的阶段进行，所以制造方法可用作可大量生产双环[3.1.0]己烷衍生物的制备方法。

2. 发明授权

US6114369A Benzimidazole compound 失效
标题翻译：苯并咪唑化合物
公开(公告)号：US6114369A
公开(公告)日：2000-09-05
申请号：US403763
申请日：1999-11-01
申请人： Keizo Tanikawa , Yoshimasa Kamikawaji , Mitsuaki Hirotsuka , Takehisa Iwama , Akiko Yamamoto , Yoichiro Fujita
发明人： Keizo Tanikawa , Yoshimasa Kamikawaji , Mitsuaki Hirotsuka , Takehisa Iwama , Akiko Yamamoto , Yoichiro Fujita
IPC分类号： A61K31/4184 , A61P37/08 , C07D235/10 , C07D235/14 , C07D235/30
CPC分类号： C07D235/14 , C07D235/30
摘要： A benzimidazole derivative of the formula (I) or its salt: wherein A is a single bond or a C.sub.1-2 alkylene group (this alkylene group may optionally be substituted by a C.sub.1-4 alkyl group), R.sup.6 is a C.sub.1-4 alkyl group (this alkyl group may optionally be substituted by a phenyl group), B is a C.sub.2-3 alkylene group (this alkylene group may optionally be substituted by a C.sub.1-4 alkyl group), X is an oxygen atom, a sulfur atom or NR.sup.7 (wherein R.sup.7 is a nitro group, a cyano group or a C.sub.1-4 alkoxy group), each of R.sup.1 and R.sup.2 which are independent of each other, is a hydrogen atom, a halogen atom, a C.sub.1-4 alkyl group or a C.sub.1-4 alkoxy group, E is a C.sub.1-2 alkylene group (this alkylene group may optionally be substituted by a C.sub.1-4 alkyl group), R.sup.3 is a phenyl group (this phenyl group may optionally be substituted by a halogen atom, a C.sub.1-4 alkyl group or a C.sub.1-4 alkoxy group), a C.sub.1-4 alkoxy group or a benzyloxy group, each of R.sup.4 and R.sup.5 which are independent of each other, is a C.sub.1-4 alkyl group (this alkyl group may optionally be substituted by a phenyl group), D is a C.sub.1-2 alkylene group (this alkylene group may optionally be substituted by a C.sub.1-4 alkyl group), and Ar is a phenyl group.
摘要翻译： PCT No.PCT / JP98 / 01986 Sec。 371日期：1999年11月1日 102（e）1999年11月1日PCT 1998年4月30日PCT PCT。 WO98 / 50368 PCT出版物日期：1998年11月12日一种式（I）的苯并咪唑衍生物或其盐：其中A为单键或C1-2亚烷基（该亚烷基可任选被C 1-4烷基取代），R 6为 C 1-4烷基（该烷基可以任选被苯基取代），B是C2-3亚烷基（该亚烷基可以任选被C 1-4烷基取代），X是氧原子，硫原子或NR 7（其中R 7为硝基，氰基或C 1-4烷氧基），R 1和R 2各自独立地为氢原子，卤素原子，C1- 4烷基或C 1-4烷氧基，E是C1-2亚烷基（该亚烷基可以任选被C 1-4烷基取代），R 3是苯基（该苯基可以任选地被卤素原子，C 1-4烷基或C 1-4烷氧基），C 1-4烷氧基或苄氧基，R 4和R 5各自独立地为C 1-4烷基（ t 其烷基可任选被苯基取代），D为C1-2亚烷基（该亚烷基可任选被C 1-4烷基取代），Ar为苯基。

3. 发明授权

US5929074A Pyridazinone derivatives with pharmaceutical activity 失效
标题翻译：具有药物活性的哒嗪酮衍生物
公开(公告)号：US5929074A
公开(公告)日：1999-07-27
申请号：US986420
申请日：1997-12-08
申请人： Keizo Tanikawa , Akira Saito , Mitsuaki Hirotsuka , Ken-ichi Shikada
发明人： Keizo Tanikawa , Akira Saito , Mitsuaki Hirotsuka , Ken-ichi Shikada
IPC分类号： C07D237/22 , A61K31/4985 , A61K31/50 , A61K31/501 , A61P7/02 , A61P11/08 , A61P37/08 , C07D237/20 , C07D401/12 , C07D403/12
CPC分类号： C07D401/12 , C07D237/20
摘要： A 3(2H)-pyridazinone derivative of the formula (I) its salt, a process for its production and a pharmaceutical composition containing it. ##STR1## wherein each of R.sup.1, R.sup.2 and R.sup.3 which are independent of one another, is a hydrogen atom or a C.sub.1-4 alkyl group, X is a chlorine atom or a bromine atom, Y.sup.1 is a hydrogen atom, a halogen atom, a nitro group, an amino group or a C.sub.1-4 alkoxy group, Y.sup.2 is a hydrogen atom, a halogen atom, a hydroxyl group, a C.sub.1-4 alkyl group or a C.sub.1-4 alkoxy group, A is a C.sub.1-5 alkylene chain which may be substituted by a hydroxyl group, B is a carbonyl group or a methylene chain which may be substituted by a C.sub.1-4 alkyl group, and each of R.sup.4 and R.sup.5 which are independent of each other, is a C.sub.1-4 alkyl group, or R.sup.4 is a hydrogen atom and R.sup.5 is --Z--Ar (wherein Z is a C.sub.1-5 alkylene chain, and Ar is an aromatic 6-membered ring which may contain a nitrogen atom), or R.sup.4 and R.sup.5 together form a C.sub.2-6 cyclic alkylene group, or R.sup.4 and R.sup.5 form together with the adjacent nitrogen atom a 4-substituted piperazine ring of the formula: ##STR2## wherein R.sup.6 is a C.sub.1-4 alkyl group.
摘要翻译：式（I）的3（2H） - 哒嗪酮衍生物及其制备方法和含有它的药物组合物。其中R 1，R 2和R 3彼此独立地为氢原子或C 1-4烷基，X为氯原子或溴原子，Y 1为氢原子，卤原子，硝基氨基或C 1-4烷氧基，Y 2是氢原子，卤素原子，羟基，C 1-4烷基或C 1-4烷氧基，A是C 1-5亚烷基链，其可以是被羟基取代，B是可被C 1-4烷基取代的羰基或亚甲基链，R 4和R 5各自独立地为C 1-4烷基，或 R4是氢原子，R5是-Z-Ar（其中Z是C1-5亚烷基链，Ar是可以含有氮原子的芳族六元环），或者R4和R5一起形成C2-6 环状亚烷基或R 4和R 5与相邻的氮原子一起形成下式的4-取代的哌嗪环：其中R 6是C 1-4烷基。

4. 发明授权

US5728702A Pyridazinone derivatives with pharmaceutical activity 失效
标题翻译：具有药物活性的哒嗪酮衍生物
公开(公告)号：US5728702A
公开(公告)日：1998-03-17
申请号：US564277
申请日：1996-03-22
申请人： Keizo Tanikawa , Akira Saito , Mitsuaki Hirotsuka , Ken-ichi Shikada
发明人： Keizo Tanikawa , Akira Saito , Mitsuaki Hirotsuka , Ken-ichi Shikada
IPC分类号： C07D237/22 , A61K31/4985 , A61K31/50 , A61K31/501 , A61P7/02 , A61P11/08 , A61P37/08 , C07D237/20 , C07D401/12 , C07D403/12 , C07D703/12
CPC分类号： C07D401/12 , C07D237/20
摘要： A 3(2H)-pyridazinone derivative of the formula (I) its salt, a process for its production and a pharmaceutical composition containing it. ##STR1## wherein each of R.sup.1, R.sup.2 and R.sup.3 which are independent of one another, is a hydrogen atom or a C.sub.1-4 alkyl group, X is a chlorine atom or a bromine atom, Y.sup.1 is a hydrogen atom, a halogen atom, a nitro group, an amino group or a C.sub.1-4 alkoxy group, Y.sup.2 is a hydrogen atom, a halogen atom, a hydroxyl group, a C.sub.1-4 alkyl group or a C.sub.1-4 alkoxy group, A is a C.sub.1-5 alkylene chain which may be substituted by a hydroxyl group, B is a carbonyl group or a methylene chain which may be substituted by a C.sub.1-4 alkyl group, and each of R.sup.4 and R.sup.5 which are independent of each other, is a C.sub.1-4 alkyl group, or R.sup.4 is a hydrogen atom and R.sup.5 is --Z--Ar (wherein Z is a C.sub.1-5 alkylene chain, and Ar is an aromatic 6-membered ring which may contain a nitrogen atom), or R.sup.4 and R.sup.5 together form a C.sub.2-6 cyclic alkylene group, or R.sup.4 and R.sup.5 form together with the adjacent nitrogen atom a 4-substituted piperazine ring of the formula: ##STR2## wherein R.sup.6 is a C.sub.1-4 alkyl group.
摘要翻译： PCT No.PCT / JP94 / 01015 Sec。 371日期：1996年3月22日 102（e）1996年3月22日PCT 1994年6月24日PCT公布。出版物WO95 / 01343 日期1995年1月12日A式（I）的3（2H） - 哒嗪酮衍生物及其制备方法和含有它的药物组合物。其中R 1，R 2和R 3彼此独立地为氢原子或C 1-4烷基，X为氯原子或溴原子，Y 1为氢原子，卤素原子，硝基，氨基或C1-4烷氧基，Y2是氢原子，卤素原子，羟基，C1-4烷基或C1-4烷氧基，A是C1 可以被羟基取代的亚烷基链，B是可以被C 1-4烷基取代的羰基或亚甲基链，并且彼此独立的R 4和R 5各自是C1 -4-烷基，或R4为氢原子，R5为-Z-Ar（其中Z为C1-5亚烷基链，Ar为可含有氮原子的芳香族6-元环）或R4和R5 一起形成C 2-6环状亚烷基，或者R 4和R 5与相邻的氮原子一起形成下式的下式的4-取代的哌嗪环：其中R 6是C 1-4烷基。

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