ARTIFICIAL AMINO ACID

Japanese Patent JP3222050

B2

PROBLEM TO BE SOLVED: To obtain a peptide strongly antagonizing against endogenous GnRH, inhibiting the internal secretion of LH and FSH and the release of steroids from the gonad of mammalian and having sufficient solubility at a pH of about 5-6.5.
SOLUTION: An artificial L or D-amino acid isomer of the formula [(i) is 1, 2 or 3; Y is N-CN, N-CONHR9 or the like; R9 is H, Ac, an alkyl, naphthyl or the like; X is NH, O, N3, M1-(CHq)P-M2 or M1-(CH2)p'-M2(CH2)p-M3; M1 is NR10, N, O or CHR3; R3 is methyl, ethyl or the like; (q) is 1 or 2: (p), (p') and (p") are each an integer of 0-6; R10 is H, methyl, ethyl or the like; M2 and M3 are each M1, COOH, CONH2 or the like; R2 is R1, OH, NH2, NHR1 or the like]. For example, the peptide having a substituted amide group at the C-terminal can be synthesized by a solid phase synthetic technique using an N-alkylaminomethyl resin.

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Hogar, Karl Aye
Revere, Gene Edward Frederick
Theobaldo, Paula Guess
John S. Porter
Kleve Lore, Revere
Vale, Wiley Walker, Juniors

JP32332595A

October 22, 2001

December 12, 1995

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THE SALK INSTITUTE FOR BIOLOGICAL STUDIES

A61K31/195; A61K31/275; A61K31/495; A61K31/505; A61K38/04; A61P5/00; A61P13/02; A61P15/00; C07C233/54; C07C233/87; C07C261/04; C07C279/24; C07C279/28; C07C327/38; C07C327/48; C07C333/08; C07C335/16; C07D209/14; C07D213/57; C07D233/64; C07D239/42; C07D241/20; C07D249/14; C07K1/113; C07K7/23; C07K14/575; A61K38/00; (IPC1-7): C07C279/24; C07C279/28; C07D233/64; C07D249/14

JP63233963A

Ｔｅｔｒａｈｅｄｒｏｎ Ｌｅｔｔｅｒｓ，Ｖｏｌ．３０，Ｎｏ．１１（１９８９）ｐ．１４０１−１４０４

Kazuo Shamoto (5 outside)

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