公开(公告)号：US4199501A

公开(公告)日：1980-04-22

申请号：US965536

申请日：1978-11-20

申请人： James E. Shields

发明人： James E. Shields

IPC分类号： A61K38/00 ,  C07K14/655 ,  C07C103/52 ,  A61K37/00

CPC分类号： C07K14/6555 ,  A61K38/00 ,  Y10S514/806 ,  Y10S930/16

摘要： Tetradecapeptides of the formula ##STR1## wherein X is H-Ala-D-Ala, H-D-Ala-Gly, or H-D-Val-Gly, and X.sup.1 is Phe or Cha, or a non-toxic pharmaceutically acceptable acid addition salt thereof, inhibit the secretion of growth hormone without materially inhibiting the secretion of glucagon or insulin. Intermediates and processes for making the tetradecapeptides are also described.

摘要翻译： 其中X是H-Ala-D-Ala，HD-Ala-Gly或HD-Val-Gly，X1是Phe或Cha或其无毒的药学上可接受的酸加成盐的式（I）的十四肽， 抑制生长激素的分泌，而不会明显抑制胰高血糖素或胰岛素的分泌。 还描述了制备十四肽的中间体和方法。

公开(公告)号：US4061607A

公开(公告)日：1977-12-06

申请号：US709465

申请日：1976-07-28

申请人： James E. Shields

发明人： James E. Shields

IPC分类号： C07K14/575 ,  A61K38/00 ,  C07K14/655 ,  C08L67/00 ,  C07C103/52

CPC分类号： C07K14/6555 ,  A61K38/00 ,  Y10S930/16 ,  Y10S930/28

摘要： The tetradecapeptides ##STR1## in which Y is L-Cha, L-Leu, or D-Phe are described along with corresponding non-toxic pharmaceutically-acceptable acid addition salts as well as intermediates useful in the synthesis of the tetradecapeptides. These tetradecapeptides as well as their pharmaceutically-acceptable acid addition salts inhibit the release of growth hormone.

摘要翻译： 其中Y是L-Cha，L-Leu或D-Phe的十四肽“IMAGE”以及相应的无毒的药学上可接受的酸加成盐以及可用于合成十四肽的中间体进行了描述。 这些十四肽及其药学上可接受的酸加成盐抑制生长激素的释放。

公开(公告)号：US4199500A

公开(公告)日：1980-04-22

申请号：US962502

申请日：1978-11-20

申请人： James E. Shields

发明人： James E. Shields

IPC分类号： A61K38/00 ,  C07K14/655 ,  C07C103/52 ,  A61K37/00

CPC分类号： C07K14/6555 ,  A61K38/00 ,  Y10S514/806 ,  Y10S930/16 ,  Y10S930/28

摘要： The tetradecapaptides of the formula ##STR1## wherein X is H-Ala-D-Ala, H-D-Ala-Gly, or H-D-Val-Gly, or the non-toxic, pharmaceutically acceptable acid addition salts thereof; inhibit the secretion of growth hormone, while not materially inhibiting the secretion of insulin or glucagon. Intermediates used in the synthesis of the tetradecapeptides are also described.

摘要翻译： 其中X是H-Ala-D-Ala，H-D-Ala-Gly或H-D-Val-Gly的式“IMAGE”的十四硫代或其无毒的药学上可接受的酸加成盐; 抑制生长激素的分泌，同时不会实质上抑制胰岛素或胰高血糖素的分泌。 还描述了用于合成十四肽的中间体。

公开(公告)号：US4076659A

公开(公告)日：1978-02-28

申请号：US667752

申请日：1976-03-17

申请人： James E. Shields

发明人： James E. Shields

IPC分类号： A61K38/00 ,  C07K14/655 ,  C07C103/52 ,  C08L37/00

CPC分类号： C07K14/655 ,  A61K38/00 ,  Y10S930/16 ,  Y10S930/28

摘要： The tetradecapeptide ##STR1## is described along with corresponding non-toxic pharmaceutically-acceptable acid addition salts as well as intermediates useful in the synthesis of the tetradecapeptide. This tetradecapeptide as well as its pharmaceutically acceptable acid addition salts inhibit the release of growth hormone and the release of gastric acid.

摘要翻译： 描述十四肽“IMAGE”以及相应的无毒的药学上可接受的酸加成盐以及可用于合成十四肽的中间体。 该十四肽及其药学上可接受的酸加成盐抑制生长激素的释放和胃酸的释放。

公开(公告)号：US4062816A

公开(公告)日：1977-12-13

申请号：US665979

申请日：1976-03-11

申请人： James E. Shields

发明人： James E. Shields

IPC分类号： A61K38/00 ,  C07K14/655 ,  C08L37/00

CPC分类号： C07K14/6555 ,  A61K38/00 ,  Y10S930/16 ,  Y10S930/28

摘要： The tetradecapeptide ##STR1## is described along with corresponding non-toxic pharmaceutically-acceptable acid addition salts as well as intermediates useful in the synthesis of the tetradecapeptide. This tetradecapeptide as well as its pharmaceutically acceptable acid addition salts inhibit the secretion of gastric acid.

摘要翻译： 描述十四肽“IMAGE”以及相应的无毒的药学上可接受的酸加成盐以及可用于合成十四肽的中间体。 该十四肽及其药学上可接受的酸加成盐抑制胃酸的分泌。

公开(公告)号：US4061626A

公开(公告)日：1977-12-06

申请号：US681640

申请日：1976-04-29

申请人： James E. Shields

发明人： James E. Shields

IPC分类号： C07K14/575 ,  A61K38/00 ,  C07K14/655 ,  C07C103/52 ,  A61K37/00

CPC分类号： C07K14/6555 ,  A61K38/00 ,  Y10S514/806 ,  Y10S930/16 ,  Y10S930/28

摘要： The tetradecapeptides ##STR1## in which Y is Gly or D-Ala are described along with corresponding non-toxic pharmaceutically-acceptable acid addition salts as well as intermediates useful in the synthesis of the tetradecapeptides. The tetradecapeptide in which Y is Gly as well as its pharmaceutically acceptable acid addition salts exhibit as their principal activity the in vivo inhibition of the release of gastric acid. The tetradecapeptide in which Y is D-Ala as well as its pharmaceutically acceptable acid addition salts exhibit as their principal activity the in vivo stimulation of the release of growth hormone.

摘要翻译： 其中Y是Gly或D-Ala的十四肽“IMAGE”以及相应的无毒的药学上可接受的酸加成盐以及可用于合成十四肽的中间体。 其中Y为Gly的十四肽及其药学上可接受的酸加成盐显示其体内抑制胃酸释放的主要活性。 其中Y是D-Ala的十四肽及其药学上可接受的酸加成盐作为其生物激素释放的体内刺激的主要活性。

公开(公告)号：US4202802A

公开(公告)日：1980-05-13

申请号：US948117

申请日：1978-10-02

申请人： James E. Shields

发明人： James E. Shields

IPC分类号： A61K38/04 ,  A61P3/00 ,  A61P3/08 ,  A61P3/10 ,  C07C231/00 ,  C07K1/113 ,  C07K14/575 ,  C07K14/655 ,  C08L89/00 ,  A61K37/00 ,  C07C103/52

CPC分类号： C07K14/6555 ,  Y10S514/806 ,  Y10S930/16

摘要： The tetradecapeptides of the formula ##STR1## wherein X is H--Ala--D--Ala, H--D--Ala--Gly, or H--D--Val--Gly; and X is Ala--Leu, Ala--Phe, Ala--D--Phe, D--Ala--Phe, or D--Ala--Cha; or the non-toxic, pharmaceutically acceptable acid addition salts thereof; inhibit secretion of growth hormone, while not materially inhibiting the secretion of insulin or glucagon. Intermediates used in the synthesis of the tetradecapeptides are also described.

摘要翻译： 其中X是H-Ala-D-Ala，H-D-Ala-Gly或H-D-Val-Gly的式“IMAGE”的十四肽; X为Ala-Leu，Ala-Phe，Ala-D-Phe，D-Ala-Phe或D-Ala-Cha; 或其无毒的药学上可接受的酸加成盐; 抑制生长激素的分泌，同时不能实质上抑制胰岛素或胰高血糖素的分泌。 还描述了用于合成十四肽的中间体。

公开(公告)号：US4100117A

公开(公告)日：1978-07-11

申请号：US789472

申请日：1977-04-21

申请人： James E. Shields

发明人： James E. Shields

IPC分类号： C07K14/575 ,  A61K38/00 ,  A61K38/10 ,  A61K38/12 ,  C07K1/04 ,  C07K14/565 ,  C07K14/655 ,  C08L37/00 ,  A61K37/00 ,  C07C103/52

CPC分类号： C07K14/6555 ,  A61K38/00 ,  Y10S930/16 ,  Y10S930/28

摘要： The tetradecapeptide ##STR1## is described along with corresponding non-toxic pharmaceutically-acceptable acid addition salts as well as intermediates useful in the synthesis of the tetradecapeptide. This tetradecapeptide as well as its pharmaceutically-acceptable acid addition salts exhibit various activities including inhibition of the release of gastric acid and reduction of gut motility.

摘要翻译： 描述了十四肽＆lt; IMA＆gt;＆gt;与相应的无毒的药学上可接受的酸加成盐以及可用于合成十四肽的中间体。 该十四肽及其药学上可接受的酸加成盐显示出各种活性，包括抑制胃酸的释放和肠道运动性的降低。

公开(公告)号：US4093574A

公开(公告)日：1978-06-06

申请号：US763943

申请日：1977-02-02

申请人： James E. Shields

发明人： James E. Shields

IPC分类号： A61K38/00 ,  C07K14/655 ,  C08L37/00 ,  A61K37/00 ,  C07C103/52

CPC分类号： C07K14/6555 ,  A61K38/00 ,  Y10S514/806 ,  Y10S930/16 ,  Y10S930/28

摘要： The tetradecapeptides ##STR1## in which Y is L-Asn or L-Ala are described along with corresponding non-toxic pharmaceutically-acceptable acid addition salts as well as intermediates useful in the synthesis of the tetradecapeptides. These tetradecapeptides as well as their pharmaceutically-acceptable acid addition salts exhibit various activities including inhibition of the release of gastric acid.