公开(公告)号：US5604210A

公开(公告)日：1997-02-18

申请号：US456723

申请日：1995-06-01

申请人： Akinobu Nagaoka ,  Tetsuji Imamoto ,  Tsuneo Asano ,  Yoshihiro Sugiura ,  Giichi Goto

发明人： Akinobu Nagaoka ,  Tetsuji Imamoto ,  Tsuneo Asano ,  Yoshihiro Sugiura ,  Giichi Goto

IPC分类号： A61K31/52 ,  A61K31/70

CPC分类号： A61K31/7076

摘要： The present invention relates to prevention or treatment a brain edema, an intracranial hemorrhage and a cerebral infarction by administering a pharmaceutically effective amount of a compound or a pharmaceutically acceptable salt thereof, for inhibiting a vascular permeability enhancer, which the compound is of the formula: ##STR1## wherein A is halogen, --X--R.sup.3 in which X is O, S, NH or NHNH, and R.sup.3 is H, acyl, a hydrocarbon group or an aromatic heterocyclic group, or --Y.dbd.R.sup.4 in which Y is N or NHN, and R.sup.4 is a divalent hydrocarbon group, and R.sup.1 is H, halogen, a hydrocarbon group, a heterocyclic group or --Z--R.sup.5 in which Z is O, S or NH, and R.sup.5 is H, a hydrocarbon group or an aromatic heterocyclic group;R.sup.2 is H, halogen, a hydrocarbon group or a heterocyclic group;B is --W--R.sup.6 in which W is CH.sub.2, CO or CS, and R.sup.6 is OH, alkoxy, acyloxy, alkylsulfinyl, alkylsulfonyl, phosphoric acid or amino, or B together with E form a cyclic phosphoric ester; andD and E are H, amino, azido, halogen or OH.

摘要翻译： 本发明涉及通过施用药学有效量的化合物或其药学上可接受的盐来抑制血管通透性增强剂来预防或治疗脑水肿，颅内出血和脑梗死，该化合物具有下式： （I）其中A是卤素，X-R 3，其中X是O，S，NH或NHNH，R 3是H，酰基，烃基或芳族杂环基，或-Y = R 4，其中 Y是N或NHN，R4是二价烃基，R1是H，卤素，烃基，杂环基或-Z-R5，其中Z是O，S或NH，R5是H，烃 基团或芳族杂环基团; R2是H，卤素，烃基或杂环基; B为-W-R 6，其中W为CH 2，CO或CS，R 6为OH，烷氧基，酰氧基，烷基亚磺酰基，烷基磺酰基，磷酸或氨基，或B与E一起形成环状磷酸酯; 并且D和E是H，氨基，叠氮基，卤素或OH。

公开(公告)号：US06774221B1

公开(公告)日：2004-08-10

申请号：US09806871

申请日：2001-05-07

申请人： Osamu Nishimura ,  Tsuneo Asano ,  Masato Suenaga ,  Hiroaki Ohmae ,  Norio Okutani

发明人： Osamu Nishimura ,  Tsuneo Asano ,  Masato Suenaga ,  Hiroaki Ohmae ,  Norio Okutani

IPC分类号： C08H100

CPC分类号： C07K1/12

摘要： A method for removing from a peptide the diketone of the methionine residue, and a method for manufacturing a peptide or salt thereof which does not possess an N-terminal methionine residue, characterized by having a peptide or salt thereof which possesses a diketone of the optionally oxidized N-terminal methionine residue react with 3,4-diaminobenzoic acid or a salt thereof in the presence of acetic acid and sodium formate, formic acid and sodium formate, or formic acid and sodium acetate.

摘要翻译： 从肽中除去甲硫氨酸残基的二酮的方法及其不具有N-末端甲硫氨酸残基的肽或其盐的制造方法，其特征在于具有肽或其盐，其具有任选的 氧化的N-末端甲硫氨酸残基与3,4-二氨基苯甲酸或其盐在乙酸和甲酸钠，甲酸和甲酸钠存在下反应，或甲酸和乙酸钠。