公开(公告)号：NZ239233A

公开(公告)日：1993-09-27

申请号：NZ23923391

申请日：1991-08-02

Applicant: HOECHST AG

Inventor： KONIG WOLFGANG ,  SANDOW JURGEN ,  KOLAR CENEK

IPC: A61K38/00 ,  A61P5/00 ,  A61P5/24 ,  C07K7/06 ,  C07K7/23 ,  C07K9/00 ,  C07K14/575 ,  A61K37/43

Abstract: Peptides of the formula in which X is alkanoyl, A is optionally substituted D-Na(2), D-Phe or D-Trp, B is optionally substituted D-Phe, C is D-Pal(3) or optionally substituted D-Phe or D-Trp, and D is Tyr or His, E is D-Ser(R ), F is Leu, Trp or Phe, G is L-Ser(R ), H is Gly-NH2, D-Ala-NH2 or azagly-NH2 and R is a glycosyl radical, have inhibitory effects on the formation of the gonadotropins lutropin and follitropin and thus also on the synthesis of testosterone and oestrogen. A process for the preparation of these peptides is described.

公开(公告)号：CZ408491A3

公开(公告)日：1993-01-13

申请号：CS408491

申请日：1991-12-27

Applicant: HOECHST AG

Inventor： KONIG WOLFGANG ,  SANDOW JURGEN KURT ,  KOLAR CENEK

IPC: A61K38/00 ,  A61K38/04 ,  A61P5/00 ,  A61P9/12 ,  C07K7/06 ,  C07K7/23 ,  C07K9/00 ,  C07K14/575 ,  A61K37/43

Abstract: The invention relates to peptides of the formula in which X is absent or is hydrogen or acyl; A is Pgl, de-hydro-Pro, Pro, D-Thi or D-Pgl or represents optionally substituted D-Nal(2), D-Phe or D-Trp; B is His or optionally substituted D-Phe; C is Trp, D-Thi, D-Pal(3) or optionally substituted D-Trp; D is Tyr, Arg of His; E is D-Ser(R1), beta -Asn, beta -Asp-OMe, D-Thi or -NH-CH(CH2R2)-CO-; F is Ser(R1), Leu, Trp or Phe; G is Gly-NH2, Aza-Gly-NH2, D-Ala-NH2 or NH-alkyl; R1 is glycosyl and R2 is hydrogen, acyl, aryl or heteroaryl. The invention also relates to methods for the preparation of these peptides, agents containing them and their use.

公开(公告)号：FI86863C

公开(公告)日：1992-10-26

申请号：FI874401

申请日：1987-10-07

Applicant: HOECHST AG

Inventor： KOENIG WOLFGANG ,  SANDOW JUERGEN KURT ,  KOLAR CENEK

IPC: A61K38/00 ,  A61K38/04 ,  A61P5/00 ,  A61P9/12 ,  C07K7/06 ,  C07K7/23 ,  C07K9/00 ,  C07K14/575

公开(公告)号：AU620184B2

公开(公告)日：1992-02-13

申请号：AU4611389

申请日：1989-12-13

Applicant: HOECHST AG

Inventor： KOLAR CENEK ,  KONIG WOLFGANG ,  SANDOW JURGEN KURT

IPC: A61K38/04 ,  A61K38/00 ,  A61P5/00 ,  C07K7/23 ,  C07K7/06 ,  C07K9/00 ,  A61K37/02

Abstract: Peptides of the formula Ac-D-Nal(2)-D-Phe-D-Phe-Ser-X-D-Ser(Rha)-Leu-Arg-Pro-Y in which X represents Tyr or His and Y represents Gly-NH2, D-Ala-NH2, Azgly-NH2 or NH-C2H5 are competitive antagonists of Gn-RH. They are used for the treatment of gonadotropin- and steroid-dependent diseases and are prepared by known methods of peptide chemistry.

公开(公告)号：NO913020L

公开(公告)日：1992-02-05

申请号：NO913020

申请日：1991-08-02

Applicant: HOECHST AG

Inventor： KOENIG WOLFGANG ,  SANDOW JUERGEN ,  KOLAR CENEK

IPC: A61K38/00 ,  A61P5/00 ,  A61P5/24 ,  C07K7/06 ,  C07K7/23 ,  C07K9/00 ,  C07K14/575

Abstract: Peptides of the formula in which X is alkanoyl, A is optionally substituted D-Na(2), D-Phe or D-Trp, B is optionally substituted D-Phe, C is D-Pal(3) or optionally substituted D-Phe or D-Trp, and D is Tyr or His, E is D-Ser(R ), F is Leu, Trp or Phe, G is L-Ser(R ), H is Gly-NH2, D-Ala-NH2 or azagly-NH2 and R is a glycosyl radical, have inhibitory effects on the formation of the gonadotropins lutropin and follitropin and thus also on the synthesis of testosterone and oestrogen. A process for the preparation of these peptides is described.

公开(公告)号：ZA899509B

公开(公告)日：1990-08-29

申请号：ZA899509

申请日：1989-12-13

Applicant: HOECHST AG

Inventor： KOLAR CENEK ,  CENEK KOLAR ,  KOENIG WOLFGANG ,  WOLFGANG KOENIG ,  SANDOW JUERGEN KURT ,  JUERGEN KURT SANDOW

IPC: A61K38/04 ,  A61K38/00 ,  A61P5/00 ,  C07K7/23 ,  C07D ,  A61K

Abstract: Peptides of the formula Ac-D-Nal(2)-D-Phe-D-Phe-Ser-X-D-Ser(Rha)-Leu-Arg-Pro-Y in which X represents Tyr or His and Y represents Gly-NH2, D-Ala-NH2, Azgly-NH2 or NH-C2H5 are competitive antagonists of Gn-RH. They are used for the treatment of gonadotropin- and steroid-dependent diseases and are prepared by known methods of peptide chemistry.

公开(公告)号：ZA8909509B

公开(公告)日：1990-08-29

申请号：ZA8909509

申请日：1989-12-13

Applicant: HOECHST AG

Inventor： KOLAR CENEK ,  CENEK KOLAR ,  KOENIG WOLFGANG ,  WOLFGANG KOENIG ,  SANDOW JUERGEN KURT ,  JUERGEN KURT SANDOW

IPC: A61K38/04 ,  A61K38/00 ,  A61P5/00 ,  C07K7/23 ,  C07D ,  A61K

CPC classification number: C07K7/23 ,  A61K38/00

公开(公告)号：CA1240319A

公开(公告)日：1988-08-09

申请号：CA485962

申请日：1985-06-28

Applicant: HOECHST AG

Inventor： THIEM JOACHIM ,  DEGER HANS-MATTHIAS ,  KOLAR CENEK ,  KREUZER MATTHIAS

IPC: C07H15/04 ,  C07H5/04

Abstract: of the disclosure: 1-Azidoaldoses are obtained by reacting 1-fluoro-aldoses with metal azides in polar, water-miscible, preferably water-containing, solvents. The hydroxyl groups do not react at the same time, so that they need not be protected or can be present in a derivatized form.

公开(公告)号：DK527187A

公开(公告)日：1988-04-10

申请号：DK527187

申请日：1987-10-08

Applicant: HOECHST AG

Inventor： KOENIG WOLFGANG ,  SANDOW JUERGEN KURT ,  KOLAR CENEK

IPC: A61K38/00 ,  A61K38/04 ,  A61P5/00 ,  A61P9/12 ,  C07K7/06 ,  C07K7/23 ,  C07K9/00 ,  C07K14/575 ,  C07K7/20

Abstract: The invention relates to peptides of the formula in which X is absent or is hydrogen or acyl; A is Pgl, de-hydro-Pro, Pro, D-Thi or D-Pgl or represents optionally substituted D-Nal(2), D-Phe or D-Trp; B is His or optionally substituted D-Phe; C is Trp, D-Thi, D-Pal(3) or optionally substituted D-Trp; D is Tyr, Arg of His; E is D-Ser(R1), beta -Asn, beta -Asp-OMe, D-Thi or -NH-CH(CH2R2)-CO-; F is Ser(R1), Leu, Trp or Phe; G is Gly-NH2, Aza-Gly-NH2, D-Ala-NH2 or NH-alkyl; R1 is glycosyl and R2 is hydrogen, acyl, aryl or heteroaryl. The invention also relates to methods for the preparation of these peptides, agents containing them and their use.

公开(公告)号：AU566580B2

公开(公告)日：1987-10-22

申请号：AU4440685

申请日：1985-06-28

Applicant: HOECHST AG

Inventor： THIEM JOACHIM ,  DEGER HANS-MATTHIAS ,  KOLAR CENEK ,  KREUZER MATTHIAS

IPC: C07H15/04 ,  C07H5/04

Abstract: 1-Azidoaldoses are obtained by reacting 1-fluoroaldoses with metal azides in polar, water-miscible, preferably water-containing, solvents. The hydroxyl groups do not react at the same time, so that they need not be protected or can be present in a derivatized form.