公开(公告)号：EP0739885A1

公开(公告)日：1996-10-30

申请号：EP95909094.5

申请日：1995-02-15

申请人： SHIONOGI & CO., LTD.

发明人： TAKADA, Susumu ,  CHOMEI, Nobuo ,  UENAKA, Masaaki

IPC分类号： C07D261/04 ,  C07D263/34

CPC分类号： C07D263/34 ,  C07D261/04 ,  C07D261/18 ,  Y02P20/55

摘要： A process for the preparation of 3-isoxazolecarboxlic acid which is an intermediate for prepearing useful compounds is provided, said process being characterized in that a compound of formula (I) is reacted with hydroxylamine to obtain a compound of formula (II), and the compound thus obtained is treated with an alkali:
wherein R 1 is a lower alkyl, R 2 is a carboxy protecting group, X is a halogen atom, and Y is a hydrogen atom, or X and Y together may form a single bond.

摘要翻译： 提供一种制备作为制备有用化合物的中间体的3-异恶唑羧酸的方法，所述方法的特征在于式（I）化合物与羟胺反应得到式（II）化合物， 由此获得的化合物用碱处理：其中R 1是低级烷基，R 2是羧基保护基，X是卤素原子，Y是氢原子，或X和Y在一起 可能形成单一债券。

公开(公告)号：EP0739885B1

公开(公告)日：2000-04-19

申请号：EP95909094.5

申请日：1995-02-15

申请人： SHIONOGI & CO., LTD.

发明人： TAKADA, Susumu ,  CHOMEI, Nobuo ,  UENAKA, Masaaki

IPC分类号： C07D261/04 ,  C07D263/34

CPC分类号： C07D263/34 ,  C07D261/04 ,  C07D261/18 ,  Y02P20/55

摘要： A process for producing 3-isoxazolecarboxylic acid as an intermediate for synthesizing valuable compounds, which comprises reacting a compound represented by general formula (I) with hydroxylamine to yield a compound represented by general formula (II) and treating the obtained compound with an alkali, wherein R1 represents lower alkyl; R2 represents a carboxyl-protecting group; and X represents halogen and Y represents hydrogen, or X and Y are combined together to form a single bond.

公开(公告)号：EP1097927A1

公开(公告)日：2001-05-09

申请号：EP99922540.2

申请日：1999-05-28

申请人： SHIONOGI & CO., LTD.

发明人： TAKADA, Susumu ,  CHOMEI, Nobuo ,  KIHARA, Tsuyoshi

IPC分类号： C07D241/44 ,  A61K31/495

CPC分类号： C07D241/52 ,  C07D241/44 ,  C07D401/04 ,  C07D403/12

摘要： A cyanoiminoquinoxaline derivative of the formula (II) is useful as a preventive or therapeutic agent for diseases due to hyperexcitation of glutamate receptors.
(wherein, X and Y each is independently O or NCN, provided that at least one of X and Y is NCN; R 1 , R 2 , R 3 , and R 4 each is independently hydrogen, halogen, nitro, optionally substituted heterocyclic group etc.; R 5 is hydrogen etc.; R 1 and R 2 , R 2 and R 3 , R 3 and R 4 , and R 4 and R 5 , each taken together with the adjacent atoms may form a carbocycle which may be substituted or may contain a heteroatom(s).)

摘要翻译： 式（II）的氰基亚氨基喹喔啉衍生物可用作谷氨酸受体过度兴奋引起的疾病的预防或治疗剂。 （其中，X和Y各自独立地为O或NCN，条件是X和Y中的至少一个为NCN; R 1，R 2，R 3和R 4各自独立地为氢，卤素，硝基，任选取代的杂环基等; R 5 是氢等; R 1和R 2，R 2和R 3，R 3和R 4，以及R 4和R 5各自与相邻原子一起可形成可被取代或可含有杂原子的碳环。）

公开(公告)号：EP1097927B1

公开(公告)日：2006-07-19

申请号：EP99922540.2

申请日：1999-05-28

申请人： SHIONOGI & CO., LTD.

发明人： TAKADA, Susumu ,  CHOMEI, Nobuo ,  KIHARA, Tsuyoshi

IPC分类号： C07D241/44 ,  A61K31/495 ,  C07D401/04

CPC分类号： C07D241/52 ,  C07D241/44 ,  C07D401/04 ,  C07D403/12

摘要： Cyanoiminoquinoxaline derivatives represented by general formula (II), which are useful as preventive or therapeutic agents for diseases due to hyperexcitation of glutamate receptors wherein X and Y are each independently O or NCN, provided at least either of X and Y is NCN; R?1, R2, R3 and R4¿ are each independently hydrogen, halogeno, nitro, an optionally substituted heterocyclic group or the like; and R5 is hydrogen or the like, or alternatively R?1 and R2, R2 and R3, R3 and R4, and R4 and R5¿ each together with the atoms adjacent thereto may form a carbocycle which may be substituted or contain a heteroatom.

摘要翻译： 至少X和Y中至少一个是NCN，由通式（II）表示的氰基亚氨基喹喔啉衍生物，其可用作由于谷氨酸受体过度兴奋引起的疾病的预防或治疗剂，其中X和Y各自独立地为O或NCN; R 1，R 2，R 3和R 4各自独立地为氢，卤素，硝基，任选取代的杂环基团等; R 5是氢等，或者R 1和R 2，R 2和R 3，R 3和R 4，以及R 4和R 5各自与与其相邻的原子一起可以形成可以被取代或含有杂原子的碳环。