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1. 发明授权

US5604226A Pyridazinone derivatives, processes for production thereof and use thereof 失效
标题翻译：哒嗪酮衍生物，其制备方法和用途
公开(公告)号：US5604226A
公开(公告)日：1997-02-18
申请号：US356510
申请日：1994-12-15
申请人： Takashi Kagawa , Takuya Motokawa , Masanori Yoshida , Yoshitami Oshita , Kazuo Kanai
发明人： Takashi Kagawa , Takuya Motokawa , Masanori Yoshida , Yoshitami Oshita , Kazuo Kanai
IPC分类号： C07D237/22 , C07D401/12 , C07D237/16
CPC分类号： C07D401/12 , C07D237/22
摘要： Pyridazinone derivatives of formula (I): ##STR1## wherein R.sup.1 represents a hydrogen atom or a methyl group which may be substituted with an aliphatic cyclic amino group optionally containing a hetero atom in the ring thereof; each of X.sup.1 and X.sup.2 independently represents a hydrogen atom, a halogen atom, an alkyl group having 1 to 6 carbon atoms, an alkoxy group having 1 to 6 carbon atoms, a cyano group, a nitro group or a group shown by --CO--NR.sup.2 R.sup.3 (wherein each of R.sup.2 and R.sup.3 independently represents an alkyl group having 1 to 6 carbon atoms); Y represents a halogen atom; Z represents an alkoxy group having 1 to 6 carbon atoms; l represents 0 or an integer of 1 to 3; A represents CH or N; m represents 0 or an integer of 1 or 2; and n represents an integer of 1 to 8, exhibit a platelet aggregation inhibiting activity and are useful for the treatment of circulatory disorders such as cerebral infarction.
摘要翻译：式（I）的哒嗪酮衍生物：其中R 1表示氢原子或可被其环中任选含有杂原子的脂族环状氨基取代的甲基; X 1和X 2各自独立地表示氢原子，卤素原子，具有1至6个碳原子的烷基，具有1至6个碳原子的烷氧基，氰基，硝基或-CO- NR2R3（其中R2和R3各自独立地表示具有1至6个碳原子的烷基）; Y表示卤原子; Z表示碳原子数1〜6的烷氧基。 l表示0或1〜3的整数， A表示CH或N; m表示0或1或2的整数; n表示1〜8的整数，表现出血小板聚集抑制活性，可用于治疗脑梗死等循环障碍。

2. 发明授权

US5981807A Production of optically active 2-halo-1-(substituted phenyl)ethanol and substituted styrene oxide 失效
标题翻译：制备光学活性2-卤代-1-（取代苯基）乙醇和取代的氧化苯乙烯
公开(公告)号：US5981807A
公开(公告)日：1999-11-09
申请号：US958333
申请日：1997-10-27
申请人： Hiroki Kodama , Takuya Motokawa , Hiroshi Yamaguchi , Masanori Yoshida
发明人： Hiroki Kodama , Takuya Motokawa , Hiroshi Yamaguchi , Masanori Yoshida
IPC分类号： C07B57/00 , C07C29/09 , C07D303/08 , C07C29/74 , C07C33/46
CPC分类号： C07D303/08 , C07B57/00 , C07C29/095 , C07B2200/07
摘要： A process for producing optically active 2-halo-1-(substituted phenyl)ethanol of a formula (Ia) or optically active styrene oxide of a formula (Ib). The process comprises the steps of reacting a compound of a formula (II) with phthalic anhydride to give a compound of a formula (III), performing optical resolution on the resulting compound using an optically active organic amine as a resolving agent, and finally performing hydrolysis or alcoholysis on the optically resolved compound (Ia) or (Ib). The scheme of the above process is: wherein X represents a halogen atom, Y represents a hydrogen atom, a halogen atom, a C.sub.1 -C.sub.6 alkyl group, a C.sub.1 -C.sub.6 alkoxy group, a C.sub.1 -C.sub.6 haloalkyl group or a C.sub.1 -C.sub.6 haloalkoxy group, Z represents a hydrogen atom, a halogen atom or a C.sub.1 -C.sub.6 alkyl group, n is 0 or an integer of 1 to 3 and m is 0 or an integer of 1 to 2. The resulting optically active compounds are useful as an intermediate for medicines.
摘要翻译：制备式（Ia）的光学活性2-卤代-1-（取代苯基）乙醇或式（Ib）的光学活性氧化苯乙烯的方法。该方法包括以下步骤：使式（II）的化合物与邻苯二甲酸酐反应，得到式（III）的化合物，使用光学活性的有机胺作为拆分剂对所得的化合物进行光学拆分，最后进行在光学拆分的化合物（Ia）或（Ib）上进行水解或醇解。上述方法的方案是：其中X表示卤素原子，Y表示氢原子，卤素原子，C1-C6烷基，C1-C6烷氧基，C1-C6卤代烷基或C1-C6 卤代烷氧基，Z表示氢原子，卤素原子或C1-C6烷基，n为0或1〜3的整数，m为0或1〜2的整数。所得光学活性化合物可用作药物中间体。

3. 发明授权

US5756862A Production of optically active 2-halo-1-(substituted phenyl)ethanol and substituted styrene oxide 失效
标题翻译：制备光学活性2-卤代-1-（取代苯基）乙醇和取代的氧化苯乙烯
公开(公告)号：US5756862A
公开(公告)日：1998-05-26
申请号：US699457
申请日：1996-08-19
申请人： Hiroki Kodama , Takuya Motokawa , Hiroshi Yamaguchi , Masanori Yoshida
发明人： Hiroki Kodama , Takuya Motokawa , Hiroshi Yamaguchi , Masanori Yoshida
IPC分类号： C07B57/00 , C07C29/09 , C07D303/08 , C07C29/74
CPC分类号： C07D303/08 , C07B57/00 , C07C29/095 , C07B2200/07
摘要： A process for producing optically active 2-halo-1-(substituted phenyl)ethanol of a formula (Ia) or optically active styrene oxide of a formula (Ib). The process comprises the steps of reacting a compound of a formula (II) with phthalic anhydride to give a compound of a formula (III), performing optical resolution on the resulting compound using an optically active organic amine as a resolving agent, and finally performing hydrolysis or alcoholysis on the optically resolved compound (Ia) or (Ib). The scheme of the above process is: ##STR1## wherein X represents a halogen atom, Y represents a hydrogen atom, a halogen atom, a C.sub.1 -C.sub.6 alkyl group, a C.sub.1 -C.sub.6 alkoxy group, a C.sub.1 -C.sub.6 haloalkyl group or a C.sub.1 -C.sub.6 haloalkoxy group, Z represents a hydrogen atom, a halogen atom or a C.sub.1 -C.sub.6 alkyl group, n is 0 or an integer of 1 to 3 and m is 0 or an integer of 1 to 2. The resulting optically active compounds are useful as an intermediate for medicines.
摘要翻译：制备式（Ia）的光学活性2-卤代-1-（取代苯基）乙醇或式（Ib）的光学活性氧化苯乙烯的方法。该方法包括以下步骤：使式（II）的化合物与邻苯二甲酸酐反应，得到式（III）的化合物，使用光学活性的有机胺作为拆分剂对所得的化合物进行光学拆分，最后进行在光学拆分的化合物（Ia）或（Ib）上进行水解或醇解。上述方法的方案是：其中X表示卤原子，Y表示氢原子，卤素原子，C1-C6烷基，C1-C6烷基，烷氧基，C1-C6卤代烷基或C1-C6卤代烷氧基，Z表示氢原子，卤素原子或C1-C6烷基，n为0或1〜3的整数，m为0或所得光学活性化合物可用作药物的中间体。

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