公开(公告)号：EP0348892A2

公开(公告)日：1990-01-03

申请号：EP89111675.8

申请日：1989-06-27

申请人： MECT CORPORATION ,  MITSUI TOATSU CHEMICALS, Inc.

发明人： Nagai, Yoshitaka ,  Shibayama, Shohei ,  Numata, Masaaki ,  Yoshimura, Shoji ,  Tanaka, Makoto ,  Ito, Masayoshi ,  Awaya, Akira ,  Kobayashi, Hisashi ,  Abe, Hayao ,  Ishizuka, Yusaku ,  Ogawa, Tomoya

IPC分类号： C07K15/00 ,  C07K9/00 ,  C07K7/06

CPC分类号： C07K9/005 ,  C07K9/001 ,  Y02P20/55

摘要： A sialic acid-bonded octapeptide represented by the following general formula (I):
wherein R represents a hydrogen atom or an acetyl group; and R′ represents a lower alkyl group, an aralkyl group, a hydrogen atom or an alkali metal atom, is herein desclosed. The peptide chain of the sialic acid-bonded octapeptide is constituted by 8 amino acid molecules on the C-terminus side of FTS and the compounds represented by formula (I) can be obtained by bonding sialic acid to the amino terminus of the peptide chain according to condensation. These octapeptides show excellent physiological activity comparable to FTS and a half life in blood longer than that of FTS and it is expected that the affinity of the peptide to lymphocytes is also enhanced. Thus they can effectively be used as medicines for treating the lowering and abnormality of functions of the thymus.

摘要翻译： 由以下通式（I）表示的唾液酸键合八肽：其中R表示氢原子或乙酰基; R min表示低级烷基，芳烷基，氢原子或碱金属原子。 唾液酸键合的八肽的肽链由FTS的C末端侧的8个氨基酸分子构成，通过将唾液酸键合到肽链的氨基末端，可以得到式（I）所示的化合物， 冷凝。 这些八肽显示与FTS相当的优异的生理活性和血液中的半衰期比FTS更长，并且预期肽对淋巴细胞的亲和力也增强。 因此，它们可以有效地用作治疗胸腺功能降低和异常的药物。

公开(公告)号：EP0425828A3

公开(公告)日：1991-09-18

申请号：EP90118901.9

申请日：1990-10-03

申请人： MITSUI TOATSU CHEMICALS, Inc.

发明人： Awaya, Akira ,  Kobayashi, Hisashi ,  Abe, Hayao

IPC分类号： A61K38/08 ,  A61K38/32

CPC分类号： A61K38/08

摘要： A medicament for prevention and remedy of disorders of decrease in the number of blood corpuscles such as leukocytes, reticuloctyes and thrombocytes (blood platelets) and the use of this medicament are disclosed. The medicament contains as an effective ingredient thereof a nonapeptide having the following amino acid sequence: pGlu-Ala-Lys-Ser-Gin-Gly-Gly-Ser-Asn or an ester or an amide at the carboxyl group of the C-terminus of the asparagine or a pharmacologically acceptable salt thereof or a derivative thereof combined with a metal. This medicament is utterly non-toxic to human and animals and effective for prevention and remedy of disorders of decrease in the number of blood corpuscles such as leucocytes caused by administration of chemotherapeutics agents such as anti-cancer agents or accompanied by cancer or viral diseases.

公开(公告)号：EP0425828A2

公开(公告)日：1991-05-08

申请号：EP90118901.9

申请日：1990-10-03

申请人： MITSUI TOATSU CHEMICALS, Inc.

发明人： Awaya, Akira ,  Kobayashi, Hisashi ,  Abe, Hayao

IPC分类号： A61K38/08 ,  A61K38/32

CPC分类号： A61K38/08

摘要： A medicament for prevention and remedy of disorders of decrease in the number of blood corpuscles such as leukocytes, reticuloctyes and thrombocytes (blood platelets) and the use of this medicament are disclosed. The medicament contains as an effective ingredient thereof a nonapeptide having the following amino acid sequence: pGlu-Ala-Lys-Ser-Gin-Gly-Gly-Ser-Asn or an ester or an amide at the carboxyl group of the C-terminus of the asparagine or a pharmacologically acceptable salt thereof or a derivative thereof combined with a metal. This medicament is utterly non-toxic to human and animals and effective for prevention and remedy of disorders of decrease in the number of blood corpuscles such as leucocytes caused by administration of chemotherapeutics agents such as anti-cancer agents or accompanied by cancer or viral diseases.

摘要翻译： 一种用于预防和血球的数量减少的病症的药物中的补救：如白细胞，reticuloctyes和血小板（血小板），并使用该药物的游离缺失盘。 所述药物含有作为在其具有下述氨基酸序列的九肽有效成分：焦谷氨酸 - 丙氨酸 - 赖氨酸 - 丝氨酸 - 谷氨酰胺 - 甘氨酸 - 甘氨酸 - 丝氨酸 - 天冬酰胺或酯或羧基基团的C-末端的酰胺 天冬酰胺或其药理学上可接受的盐或其衍生物与金属结合。 此药物是完全无毒的对人和动物和有效用于血球的数量减少的疾病的预防和补救：诸如通过化疗剂的给药引起的白细胞：如抗癌剂或癌症或病毒疾病的陪同下。