公开(公告)号：CA2075558C

公开(公告)日：2003-03-18

申请号：CA2075558

申请日：1992-08-07

Applicant: HOECHST AG

Inventor： ROSCHER GUNTER ,  KLEINER HANS-JERG ,  BERGER HARALD ,  SCHMIDT MANFRED ,  UHMANN RAINER ,  BOTTGER DIRK

IPC: C07F9/48 ,  C07F9/38 ,  C08G79/02 ,  C08G79/04

Abstract: Process for the preparation of pure propanephosphonic anhydride, which comprises distilling crude, impure propanephosphonic anhydride having an average degree of polymerization of 20 to 200 and containing less than 0.5% by weight of water by heating to 230 to 300.degree.C under a pressure of 0.1 to 100 mbar, pure propanephosphonic anhydride having an average decree of polymerization of 20 to 60 being obtained.

公开(公告)号：CA1156217A

公开(公告)日：1983-11-01

申请号：CA357096

申请日：1980-07-25

Applicant: HOECHST AG

Inventor： OBERMEIER RAINER ,  UHMANN RAINER ,  SUMM HANS-DIETER ,  REGITZ GUENTER ,  GEISEN KARL

IPC: C08H1/00 ,  A61K38/28 ,  A61P3/08 ,  A61P3/10 ,  C07K1/113 ,  C07K14/575 ,  C07K14/62 ,  C08G65/00 ,  C08G65/32 ,  C07C103/52

Abstract: HOE 79/F 208 NOVEL INSULIN DERIVATIVES AND PROCESS FOR THE PREPARATION THEREOF of the disclosure: Subject of the invention is an insulin derivative the alpha-amino group of the B-chain of which is linked to monoalkyl-polyethyleneglycol via a connecting member; a process for the preparation thereof, its use for the treatment of diabetes mellitus, and a medicament containing this insulin derivative.

公开(公告)号：DK170820B1

公开(公告)日：1996-01-29

申请号：DK137085

申请日：1985-03-26

Applicant: HOECHST AG

Inventor： UHMANN RAINER ,  RADSCHEIT KURT

IPC: C07K5/08 ,  A61K38/00 ,  C07K5/06 ,  C07K5/097 ,  C07K7/06 ,  C07K7/23 ,  C07K14/575

Abstract: The invention relates to a process for the preparation of peptides of the formula I U-A1-A213 A3-A4-A5-X (I) in which U denotes a urethane protective group, A1 denotes Trp or D-Trp, A2 denotes Ser, Ala or Thr, A3 denotes Tyr or Phe, A4 denotes Gly, the residue of a D-amino acid or the residue of a D-amino acid derivative, A5 denotes Leu, N-methyl-Leu, N-ethyl-Leu, Ser(But), Cys(But), Asp(OBut), Glu(OBut), Orn(Boc) or Lys(Boc) and X denotes OBut or A6-Pro-Y, where A6 represents Arg, Orn, Lys or homoarginine, and Y represents Gly-NH2, NH-NH-CO-NH2, (C1-C3)-alkylamino, cyclopropylamino, (C1-C3)-alkylamino which is substituted with hydroxyl or fluorine, or cycloalkylamino which is substituted with hydroxyl or fluorine, using tripeptides of the formula II, U-A1-A2-A3-OH, in which the residues are defined as above. The invention also relates to peptides of the formula II as intermediates in this process.

公开(公告)号：CA2075558A1

公开(公告)日：1993-02-09

申请号：CA2075558

申请日：1992-08-07

Applicant: HOECHST AG

Inventor： ROSCHER GUENTER ,  KLEINER HANS-JERG ,  BERGER HARALD ,  SCHMIDT MANFRED ,  UHMANN RAINER ,  BOETTGER DIRK

IPC: C07F9/48 ,  C07F9/38 ,  C08G79/02 ,  C08G79/04

Abstract: Process for the preparation of pure propanephosphonic anhydride, which comprises distilling crude, impure propanephosphonic anhydride having an average degree of polymerization of 20 to 200 and containing less than 0.5% by weight of water by heating to 230 to 300.degree.C under a pressure of 0.1 to 100 mbar, pure propanephosphonic anhydride having an average decree of polymerization of 20 to 60 being obtained.

公开(公告)号：HU197928B

公开(公告)日：1989-06-28

申请号：HU103285

申请日：1985-03-20

Applicant: HOECHST AG

Inventor： UHMANN RAINER ,  RADSCHEIT KURT

IPC: C07K5/08 ,  A61K38/00 ,  C07K5/06 ,  C07K5/097 ,  C07K7/06 ,  C07K7/23 ,  C07K14/575

Abstract: The invention relates to a process for the preparation of peptides of the formula I U-A1-A213 A3-A4-A5-X (I) in which U denotes a urethane protective group, A1 denotes Trp or D-Trp, A2 denotes Ser, Ala or Thr, A3 denotes Tyr or Phe, A4 denotes Gly, the residue of a D-amino acid or the residue of a D-amino acid derivative, A5 denotes Leu, N-methyl-Leu, N-ethyl-Leu, Ser(But), Cys(But), Asp(OBut), Glu(OBut), Orn(Boc) or Lys(Boc) and X denotes OBut or A6-Pro-Y, where A6 represents Arg, Orn, Lys or homoarginine, and Y represents Gly-NH2, NH-NH-CO-NH2, (C1-C3)-alkylamino, cyclopropylamino, (C1-C3)-alkylamino which is substituted with hydroxyl or fluorine, or cycloalkylamino which is substituted with hydroxyl or fluorine, using tripeptides of the formula II, U-A1-A2-A3-OH, in which the residues are defined as above. The invention also relates to peptides of the formula II as intermediates in this process.

公开(公告)号：HUT37445A

公开(公告)日：1985-12-28

申请号：HU103285

申请日：1985-03-20

Applicant: HOECHST AG

Inventor： UHMANN RAINER ,  RADSCHEIT KURT

IPC: C07K5/08 ,  A61K38/00 ,  C07K5/06 ,  C07K5/097 ,  C07K7/06 ,  C07K7/23 ,  C07K14/575 ,  C07K7/20

Abstract: The invention relates to a process for the preparation of peptides of the formula I U-A1-A213 A3-A4-A5-X (I) in which U denotes a urethane protective group, A1 denotes Trp or D-Trp, A2 denotes Ser, Ala or Thr, A3 denotes Tyr or Phe, A4 denotes Gly, the residue of a D-amino acid or the residue of a D-amino acid derivative, A5 denotes Leu, N-methyl-Leu, N-ethyl-Leu, Ser(But), Cys(But), Asp(OBut), Glu(OBut), Orn(Boc) or Lys(Boc) and X denotes OBut or A6-Pro-Y, where A6 represents Arg, Orn, Lys or homoarginine, and Y represents Gly-NH2, NH-NH-CO-NH2, (C1-C3)-alkylamino, cyclopropylamino, (C1-C3)-alkylamino which is substituted with hydroxyl or fluorine, or cycloalkylamino which is substituted with hydroxyl or fluorine, using tripeptides of the formula II, U-A1-A2-A3-OH, in which the residues are defined as above. The invention also relates to peptides of the formula II as intermediates in this process.

公开(公告)号：CA1278650C

公开(公告)日：1991-01-02

申请号：CA477529

申请日：1985-03-26

Applicant: HOECHST AG

Inventor： UHMANN RAINER ,  RADSCHEIT KURT

IPC: C07K5/08 ,  A61K38/00 ,  C07K5/06 ,  C07K5/097 ,  C07K7/06 ,  C07K7/23 ,  C07K14/575 ,  A61K37/02

Abstract: The invention relates to a process for the preparation of peptides of the formula I U - A1 - A2 - A3 - A4 - A5 - X (I) in which U denotes a urethane protective group, A1 denotes Trp or D-Trp, A2 denotes Ser, Ala or Thr, A denotes Tyr or Phe, A4 denotes Gly, the residue of a D-amino acid or the residue of a D-amino acid derivative, A5 denotes Leu, N-methyl-Leu, N-ethyl-Leu, Ser(But), Cys(But), Asp(OBut), Glu(OBut), Orn(Boc) or Lys(Boc) and X denotes OBut or A6-Pro-Y, where A6 represents Arg, Orn, Lys or homoarginine, and Y repre-sents Gly-NH2, NH-NH-CO-NH2, (C1-C3)-alkylamino, cyclopropylamino, (C1-C3)-alkylamino which is substituted with hydroxyl or fluorine, or cycloalkylamino which is substituted with hydroxyl or fluorine, using tripeptides of the formula II, U - A1 - A2 - A3 - OH, in which the residues are defined as above. The invention also relates to peptides of the formula II as intermediates in this process.

公开(公告)号：DK137085A

公开(公告)日：1985-09-28

申请号：DK137085

申请日：1985-03-26

Applicant: HOECHST AG

Inventor： UHMANN RAINER ,  RADSCHEIT KURT

IPC: C07K5/08 ,  A61K38/00 ,  C07K5/06 ,  C07K5/097 ,  C07K7/06 ,  C07K7/23 ,  C07K14/575 ,  C07K

Abstract: The invention relates to a process for the preparation of peptides of the formula I U-A1-A213 A3-A4-A5-X (I) in which U denotes a urethane protective group, A1 denotes Trp or D-Trp, A2 denotes Ser, Ala or Thr, A3 denotes Tyr or Phe, A4 denotes Gly, the residue of a D-amino acid or the residue of a D-amino acid derivative, A5 denotes Leu, N-methyl-Leu, N-ethyl-Leu, Ser(But), Cys(But), Asp(OBut), Glu(OBut), Orn(Boc) or Lys(Boc) and X denotes OBut or A6-Pro-Y, where A6 represents Arg, Orn, Lys or homoarginine, and Y represents Gly-NH2, NH-NH-CO-NH2, (C1-C3)-alkylamino, cyclopropylamino, (C1-C3)-alkylamino which is substituted with hydroxyl or fluorine, or cycloalkylamino which is substituted with hydroxyl or fluorine, using tripeptides of the formula II, U-A1-A2-A3-OH, in which the residues are defined as above. The invention also relates to peptides of the formula II as intermediates in this process.

公开(公告)号：DK137085D0

公开(公告)日：1985-03-26

申请号：DK137085

申请日：1985-03-26

Applicant: HOECHST AG

Inventor： UHMANN RAINER ,  RADSCHEIT KURT

IPC: C07K5/08 ,  A61K38/00 ,  C07K5/06 ,  C07K5/097 ,  C07K7/06 ,  C07K7/23 ,  C07K14/575 ,  C07K

Abstract: The invention relates to a process for the preparation of peptides of the formula I U-A1-A213 A3-A4-A5-X (I) in which U denotes a urethane protective group, A1 denotes Trp or D-Trp, A2 denotes Ser, Ala or Thr, A3 denotes Tyr or Phe, A4 denotes Gly, the residue of a D-amino acid or the residue of a D-amino acid derivative, A5 denotes Leu, N-methyl-Leu, N-ethyl-Leu, Ser(But), Cys(But), Asp(OBut), Glu(OBut), Orn(Boc) or Lys(Boc) and X denotes OBut or A6-Pro-Y, where A6 represents Arg, Orn, Lys or homoarginine, and Y represents Gly-NH2, NH-NH-CO-NH2, (C1-C3)-alkylamino, cyclopropylamino, (C1-C3)-alkylamino which is substituted with hydroxyl or fluorine, or cycloalkylamino which is substituted with hydroxyl or fluorine, using tripeptides of the formula II, U-A1-A2-A3-OH, in which the residues are defined as above. The invention also relates to peptides of the formula II as intermediates in this process.