公开(公告)号：EP0933379A1

公开(公告)日：1999-08-04

申请号：EP97935856.1

申请日：1997-08-22

申请人： SHIONOGI & CO., LTD.

发明人： SUGAWARA, Tamio ,  YOSHIKAWA, Takayoshi ,  TADA, Yukio

IPC分类号： C07K5/078 ,  C07K5/097 ,  C07D417/06 ,  C07D277/02 ,  A61K38/06

CPC分类号： C07D417/06 ,  A61K38/00 ,  C07D207/28 ,  C07D277/24 ,  C07D417/14 ,  C07K5/0202 ,  C07K5/06139 ,  C07K5/0821 ,  C07K5/0825 ,  C07K5/1024

摘要： The compounds having superior activity to known TRH and its derivatives in view of the activation of the central nervous system, for example, sustained acetylcholine releasing action, anti-reserpine action and locomotor increment activity was provided.
A peptide derivative of the formula (I):
, its pharmaceutically acceptable salt, or hydrate thereof.

摘要翻译： 考虑到中枢神经系统的活化，具有对已知TRH及其衍生物具有优异活性的化合物，例如维持乙酰胆碱释放作用，抗利血平作用和运动增量活性。 式（I）的肽衍生物：其化学上可接受的盐或其水合物

公开(公告)号：EP0893442B1

公开(公告)日：2005-01-12

申请号：EP97907316.0

申请日：1997-03-14

申请人： SHIONOGI & CO., LTD.

发明人： AONO, Katsutoshi ,  ICHIHASHI, Teruhisa ,  SUGAWARA, Tamio ,  HIRANO, Koichiro

IPC分类号： C07D233/84 ,  C07D401/06 ,  A61K31/415

CPC分类号： C07D401/06 ,  A61K31/415 ,  C07D233/84

摘要： Compounds represented by general formula (I), which can be absorbed efficiently through lymph vessels in the intestinal tract and migrate to lymph nodes in high concentrations, salts and hydrates thereof, and anti-AIDS agents containing the same. In said formula, Z represents S, SO, SO2, or CH2; and R represents a group represented by general formulae (Ia) and (Ib) wherein R1 represents optionally susbtituted lower alkyl; R2 represents optionally substituted lower alkyl, lower alkenyl, cycloalkylalkyl, lower aroylalkyl, aralkyl, heteroarylalkyl or carbamoyloxyalkyl; A represents lower alkylene which may have an intervening heteroatom; and R3 represents (1) C¿11?-C20 alklyl, (2) acyloxyalkyl, (3) -CR?4R5(OR6¿), (4) -C(=CR7R8)R9, (5) -COR10, (6) -COOR13, (7) -CONHCOR14, (8) -CONHCOOR15, or (9) -CONHCH¿2?NR16R17.

公开(公告)号：EP0893442A1

公开(公告)日：1999-01-27

申请号：EP97907316.0

申请日：1997-03-14

申请人： SHIONOGI & CO., LTD.

发明人： AONO, Katsutoshi ,  ICHIHASHI, Teruhisa ,  SUGAWARA, Tamio ,  HIRANO, Koichiro

IPC分类号： C07D233/84 ,  A61K31/415

CPC分类号： C07D401/06 ,  A61K31/415 ,  C07D233/84

摘要： A compound of the formula (I):
wherein X, Y, Z and R are as defined above,
salt thereof, or hydrate thereof which effectively be absorbed from the lymph vessel in the intestinal tract and transferred to the lymph node in a high concentration is provided.

摘要翻译： 式（I）化合物：其中X，Y，Z和R如上定义，其盐或其水合物，其有效地从肠道中的淋巴管吸收并转移到淋巴结中 提供了高浓度。

公开(公告)号：EP0933379B1

公开(公告)日：2006-03-22

申请号：EP97935856.1

申请日：1997-08-22

申请人： SHIONOGI & CO., LTD.

发明人： SUGAWARA, Tamio ,  YOSHIKAWA, Takayoshi ,  TADA, Yukio

IPC分类号： C07K5/078 ,  C07K5/097 ,  C07D417/06 ,  C07D277/02 ,  A61K38/06 ,  C07K5/06 ,  C07K5/08 ,  A61K38/05

CPC分类号： C07D417/06 ,  A61K38/00 ,  C07D207/28 ,  C07D277/24 ,  C07D417/14 ,  C07K5/0202 ,  C07K5/06139 ,  C07K5/0821 ,  C07K5/0825 ,  C07K5/1024

摘要： Peptide derivatives represented by general formula (I), pharmacologically acceptable salts thereof or hydrates of the same having improved central activating effects such as sustained acetylcholine-releasing effect, antireserpine effect and spontaneous motility increasing effect as compared with the publicly known TRH and TRH derivatives.