公开(公告)号：EP1132094A1

公开(公告)日：2001-09-12

申请号：EP99972107.9

申请日：1999-11-12

申请人： SHIONOGI & CO., LTD.

发明人： SUGITA, Katsuji ,  NISHIHARA, Yoshitaka ,  YOSHIKAWA, Takanori ,  KIHARA, Tsuyoshi

IPC分类号： A61K45/00 ,  A61K31/44 ,  A61K47/10 ,  A61K47/14

CPC分类号： A61K47/14 ,  A61K9/0014 ,  A61K31/437 ,  A61K47/10

摘要： Percutaneously administrable preparations which each comprise either an aqueous base comprising 1-menthol, a lower alcohol, and an acidic buffer or water, or an oily base comprising 1-menthol, a lower alcohol, and isopropyl myristate, and a cerebral function activator selected from among, e.g., 2-(3-isoxazolyl)-3,6,7,9-tetrahydroimidazo[4,5-d]pyrano[4,3-b]pyridine, salts of the same, and hydrates of both.

摘要翻译： 包含1-薄荷醇，低级醇和酸性缓冲液或水的水性基质或包含1-薄荷醇，低级醇和肉豆蔻酸异丙酯的油性基质的经皮给药的制剂和选自以下的大脑功能活化剂 例如2-（3-异恶唑基）-3,6,7,9-四氢咪唑并[4,5-d“吡喃并[4,3-b]吡啶，其盐和两者的水合物。

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。

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。）