公开(公告)号：US20080306242A1

公开(公告)日：2008-12-11

申请号：US12189925

申请日：2008-08-12

Applicant: Jon H. Rasmussen ,  Palle H. Rasmussen ,  Wolfgang O. Wachs ,  Stefan Hansen ,  Jens Fomsgaard

Inventor： Jon H. Rasmussen ,  Palle H. Rasmussen ,  Wolfgang O. Wachs ,  Stefan Hansen ,  Jens Fomsgaard

IPC: C07K7/23 ,  C07K1/00 ,  C07K5/00

CPC classification number: C07K7/23 ,  C07K1/02 ,  C07K5/0827

Abstract: The peptides Ac-D-2Nal-D-4ClPhe-D-3Pal-OH and Boc-D-2Nal-D-4ClPhe-D-3Pal-OH are intermediates useful in the synthesis of LHRH analogs by coupling with suitable heptapeptides, in particular with the heptapeptides P1-Ser(P2)-MMeTry(P3)-D-Lys(Nic)-Leu-Lys(iPr,P4)-Pro-D-AlaNH2 and P1-Ser(P2)-NMeTry(P3)-D-Asn-Leu-Lys(iPr,P4)-Pro-D-AlaNH2.

Abstract translation: 肽Ac-D-2Nal-D-4ClPhe-D-3Pal-OH和Boc-D-2Nal-D-4ClPhe-D-3Pal-OH是通过与合适的七肽偶合合成LHRH类似物的中间体，特别是 与七肽P1-Ser（P2）-MeTry（P3）-D-Lys（Nic）-Leu-Lys（iPr，P4）-Pro-D-AlaNH2和P1-Ser（P2）-NMeTry（P3）-D -Asn-Leu-Lys（iPr，P4）-Pro-D-AlaNH 2。

公开(公告)号：US07057014B2

公开(公告)日：2006-06-06

申请号：US10500302

申请日：2002-12-23

Applicant: Jon H. Rasmussen ,  Palle H. Rasmussen

Inventor： Jon H. Rasmussen ,  Palle H. Rasmussen

IPC: A61K38/08

CPC classification number: C07K7/06 ,  C07K1/30

Abstract: A nona- or decapeptide is purified from residual organic solvent by dissolving in a solvent comprising water and at least one C1–C3 alcohol followed by precipitation into a vigorously stirred solvent consisting of an alkyl ester of a carboxylic acid, the ester comprising from 3 to 6 carbon atoms, and one or several non-polar compounds selected from hexane, heptane, octane, cyclohexane, methylcyclohexane, and, optionally, of up to 5% of acetic or propionic acid, isolating the precipitated nona- or decapeptide, followed by washing with a mixture of C3–C5 esters and drying, with the provisio that the water content of the solvent comprising water and the at least one alcohol is below 8% (v/v), and that the volume ratio of the dissolution solvent mixture and the precipitation solvent mixture is 1:10 or higher. Also described is the monoacetate of Ac-D-2Nal-D-4ClPhe-D-3Pal-Ser-MeTyr-D-Asn-Leu-Lys(iPr)-Pro-D-Ala-NH2.

Abstract translation: 通过将溶解在包含水和至少一种C 1 -C 3 - 醇的溶剂中，然后沉淀到剧烈搅拌的溶剂中，从残留的有机溶剂中纯化非肽或十肽 由羧酸的烷基酯，包含3至6个碳原子的酯和选自己烷，庚烷，辛烷，环己烷，甲基环己烷中的一种或几种非极性化合物，和任选地至多5％ 乙酸或丙酸，分离沉淀的非 - 或十肽，然后用C 3 -C 5 - 酯的混合物洗涤并干燥，条件是水含量 包含水和至少一种醇的溶剂的含量低于8％（v / v），溶解溶剂混合物和沉淀溶剂混合物的体积比为1:10或更高。 还描述了Ac-D-2Nal-D-4ClPhe-D-3Pal-Ser-MeTyr-D-Asn-Leu-Lys（iPr）-Pro-D-Ala-NH 2 。

公开(公告)号：US08173770B2

公开(公告)日：2012-05-08

申请号：US12189925

申请日：2008-08-12

Applicant: Jon H. Rasmussen ,  Palle H. Rasmussen ,  Wolfgang O. Wachs ,  Stefan Hansen ,  Jens Fomsgaard

Inventor： Jon H. Rasmussen ,  Palle H. Rasmussen ,  Wolfgang O. Wachs ,  Stefan Hansen ,  Jens Fomsgaard

IPC: A61K38/06 ,  A61K38/08 ,  A61K38/24 ,  C07K1/06

CPC classification number: C07K7/23 ,  C07K1/02 ,  C07K5/0827

Abstract: The peptides Ac-D-2Nal-D-4ClPhe-D-3Pal-OH and Boc-D-2Nal-D-4ClPhe-D-3Pal-OH are intermediates useful in the synthesis of LHRH analogs by coupling with suitable heptapeptides, in particular with the heptapeptides P1-Ser(P2)-MMeTry(P3)-D-Lys(Nic)-Leu-Lys(iPr,P4)-Pro-D-AlaNH2 and P1-Ser(P2)-NMeTry(P3)-D-Asn-Leu-Lys(iPr,P4)-Pro-D-AlaNH2.

Abstract translation: 肽Ac-D-2Nal-D-4ClPhe-D-3Pal-OH和Boc-D-2Nal-D-4ClPhe-D-3Pal-OH是通过与合适的七肽偶合合成LHRH类似物的中间体，特别是 与七肽P1-Ser（P2）-MeTry（P3）-D-Lys（Nic）-Leu-Lys（iPr，P4）-Pro-D-AlaNH2和P1-Ser（P2）-NMeTry（P3）-D -Asn-Leu-Lys（iPr，P4）-Pro-D-AlaNH 2。