公开(公告)号：CY2119B1

公开(公告)日：2002-04-26

申请号：CY9800037

申请日：1998-09-29

Applicant: HOECHST AG

Inventor： ENHSEN ALFONS DR ,  GLOMBIK HEINER DR ,  KRAMER WERNER DR ,  WESS GUENTER DR

IPC: A61K31/575 ,  A61K31/58 ,  A61K31/675 ,  A61P3/06 ,  A61P9/10 ,  C07J9/00 ,  C07J17/00 ,  C07J41/00 ,  C07J43/00

Abstract: Tetrazole bile acid derivatives of the formula I G1 - X - G2 I in which G1, G2 and X have the stated meanings, and processes for their preparation are described. The compounds have valuable pharmacological properties and can therefore be used as medicines.

公开(公告)号：DK0417725T3

公开(公告)日：1997-11-03

申请号：DK90117470

申请日：1990-09-11

Applicant: HOECHST AG

Inventor： KRAMER WERNER DR ,  WESS G

IPC: A61K38/00 ,  A61K31/575 ,  A61K31/58 ,  A61P1/16 ,  A61P3/06 ,  A61P43/00 ,  C07D213/26 ,  C07D213/56 ,  C07D213/81 ,  C07J9/00 ,  C07J17/00 ,  C07J31/00 ,  C07J41/00 ,  C07J43/00 ,  C07J51/00 ,  C07K5/06 ,  C07K5/062

Abstract: Bile acid derivatives of the formula I W-X-G in which G is a bile acid residue, W is an active substance portion of a medicament and X is a linker between bile acid residue and active substance portion, are outstandingly suitable for introducing active substances into the enterohepatic circulation. The compounds I are absorbed and enter the bloodstream. This makes it possible by utilising the natural reabsorption of the bile acids to improve the absorption of drugs which are absorbed with difficulty, if at all. W can be, for example, a peptide, an antibiotic, an antiviral substance, an anticancer agent, a liver protective, an antihyperlipidaemic, a diuretic, an agent to lower blood pressure, a renin inhibitor, a substance to treat cirrhosis of the liver or a substance for treating diabetes. G is a bile acid residue in the form of the free, natural or chemically modified acids, the esters and amides, the salt forms and forms derivatised on alcohol groups. X is a large number of intermediate members or else a bond.

公开(公告)号：CZ113493A3

公开(公告)日：1994-01-19

申请号：CZ113493

申请日：1993-06-10

Applicant: HOECHST AG

Inventor： ENHSEN ALFONS DR ,  GLOMBIK HEINER DR ,  KRAMER WERNER DR ,  WESS GUNTHER DR

IPC: A61K31/575 ,  A61P1/00 ,  A61P3/00 ,  A61P3/06 ,  A61P7/00 ,  C07H9/00 ,  C07J9/00 ,  C07J41/00

Abstract: Bile acid derivatives of the formula I Z(X-GS)n in which GS, X, Z and n have the stated meanings, and a process for the production of these compounds are described. The compounds have pharmacological activity and can therefore be used as pharmaceuticals, in particular as hypolipidaemic.

公开(公告)号：CY2112B1

公开(公告)日：2002-04-26

申请号：CY9800029

申请日：1998-09-29

Applicant: HOECHST AG

Inventor： KRAMER WERNER DR ,  WESS GUENTHER DR

IPC: A61K38/00 ,  A61K31/575 ,  A61K31/58 ,  A61P1/16 ,  A61P3/06 ,  A61P43/00 ,  C07D213/26 ,  C07D213/56 ,  C07D213/81 ,  C07J9/00 ,  C07J17/00 ,  C07J31/00 ,  C07J41/00 ,  C07J43/00 ,  C07J51/00 ,  C07K5/06 ,  C07K5/062

Abstract: Bile acid derivatives of the formula I W-X-G in which G is a bile acid residue, W is an active substance portion of a medicament and X is a linker between bile acid residue and active substance portion, are outstandingly suitable for introducing active substances into the enterohepatic circulation. The compounds I are absorbed and enter the bloodstream. This makes it possible by utilising the natural reabsorption of the bile acids to improve the absorption of drugs which are absorbed with difficulty, if at all. W can be, for example, a peptide, an antibiotic, an antiviral substance, an anticancer agent, a liver protective, an antihyperlipidaemic, a diuretic, an agent to lower blood pressure, a renin inhibitor, a substance to treat cirrhosis of the liver or a substance for treating diabetes. G is a bile acid residue in the form of the free, natural or chemically modified acids, the esters and amides, the salt forms and forms derivatised on alcohol groups. X is a large number of intermediate members or else a bond.

公开(公告)号：CZ285104B6

公开(公告)日：1999-05-12

申请号：CZ113493

申请日：1993-06-10

Applicant: HOECHST AG

Inventor： ENHSEN ALFONS DR ,  GLOMBIK HEINER DR ,  KRAMER WERNER DR ,  WESS GUNTHER DR

IPC: A61K31/575 ,  A61P1/00 ,  A61P3/00 ,  A61P3/06 ,  A61P7/00 ,  C07H9/00 ,  C07J9/00 ,  C07J41/00

Abstract: Bile acid derivatives of the formula I Z(X-GS)n in which GS, X, Z and n have the stated meanings, and a process for the production of these compounds are described. The compounds have pharmacological activity and can therefore be used as pharmaceuticals, in particular as hypolipidaemic.

公开(公告)号：DK0489423T3

公开(公告)日：1997-04-14

申请号：DK91120841

申请日：1991-12-04

Applicant: HOECHST AG

Inventor： WESS G, GUENTHER, DR. ,  KRAMER WERNER DR ,  MUELLER STEFAN DR. ,  NEUBAUER HORST DR

IPC: A61K31/575 ,  A61K31/58 ,  A61P3/06 ,  C07J9/00 ,  C07J31/00 ,  C07J41/00 ,  C07J43/00

Abstract: The invention relates to bile acid derivatives of the formula I G1-X-G2(I) in which G1 and G2 are bile acid radicals or modified bile acid radicals in the form of the free acids, the esters or amides, the salt forms and also the forms derivatized on the alcohol groups and X is a bridge group or a single covalent bond, it being possible for G1 and G2 to be optionally bonded via X. The compounds according to the invention have a high affinity for the specific bile acid transport system of the small intestine and inhibit bile acid absorption in a concentration-dependent and competitive manner.

公开(公告)号：DE3930696A1

公开(公告)日：1991-03-28

申请号：DE3930696

申请日：1989-09-14

Applicant: HOECHST AG

Inventor： KRAMER WERNER DR ,  WESS GUENTHER DR

IPC: A61K38/00 ,  A61K31/575 ,  A61K31/58 ,  A61P1/16 ,  A61P3/06 ,  A61P43/00 ,  C07D213/26 ,  C07D213/56 ,  C07D213/81 ,  C07J9/00 ,  C07J17/00 ,  C07J31/00 ,  C07J41/00 ,  C07J43/00 ,  C07J51/00 ,  C07K5/06 ,  C07K5/062

Abstract: Bile acid derivatives of the formula I W-X-G in which G is a bile acid residue, W is an active substance portion of a medicament and X is a linker between bile acid residue and active substance portion, are outstandingly suitable for introducing active substances into the enterohepatic circulation. The compounds I are absorbed and enter the bloodstream. This makes it possible by utilising the natural reabsorption of the bile acids to improve the absorption of drugs which are absorbed with difficulty, if at all. W can be, for example, a peptide, an antibiotic, an antiviral substance, an anticancer agent, a liver protective, an antihyperlipidaemic, a diuretic, an agent to lower blood pressure, a renin inhibitor, a substance to treat cirrhosis of the liver or a substance for treating diabetes. G is a bile acid residue in the form of the free, natural or chemically modified acids, the esters and amides, the salt forms and forms derivatised on alcohol groups. X is a large number of intermediate members or else a bond.

公开(公告)号：DE3924506A1

公开(公告)日：1991-01-31

申请号：DE3924506

申请日：1989-07-25

Applicant: HOECHST AG

Inventor： KLEEMANN HEINZ-WERNER DR ,  URBACH HANSJOERG DR ,  WAGNER ADALBERT DR ,  RUPPERT DIETER DR ,  LINZ WOLFGANG DR ,  KRAMER WERNER DR

IPC: C07C237/08 ,  C07C237/22 ,  C07D233/54 ,  C07D401/12 ,  C07D403/12 ,  C07D409/12 ,  C07K5/065 ,  C07K5/078

Abstract: Peptide polyhydroxyalkylamides of formula (I) and their salts are new; where A = R1R6N-CHR5-CO-, R1R7CH-CHR5-CO- or R1O-CHR5-CO-; R1 = R'1 or R'1W; R'1 = (a) 3-8C cycloalkyl, CONH2, OCH2COOH, NH2, etc. (b) H, OH or 1-4C alkoxy, (c) 1-18C alkyl, quanidino, phenyl(1-4C)alkoxy, etc. (d) 6-14C aryl, (6-14C)aryl(1-4C)alkyl, etc. (e) Het or Het(1-4C)alkyl, where Het is an opt. benzo-fused 5- to 7-membered heterocyclic ring contg. 1 or 2 of N, O, S, No, etc. (f) NR8R9; Het or Het(1-4C)alkyl, or NR8R9 is a mono- or bicyclic 5- to 12-membered ring system opt. contg. 1 or 2 more N atoms, an S atom or an O atom, opt. substd. by 1-4C alkyl; W = CO, CS, OSO, SO2, SO, NHSO2, NHCO, CHOH or NOH; n = 2-10.

公开(公告)号：DE59010706D1

公开(公告)日：1997-05-28

申请号：DE59010706

申请日：1990-09-11

Applicant: HOECHST AG

Inventor： KRAMER WERNER DR ,  WESS GUENTHER DR

IPC: A61K38/00 ,  A61K31/575 ,  A61K31/58 ,  A61P1/16 ,  A61P3/06 ,  A61P43/00 ,  C07D213/26 ,  C07D213/56 ,  C07D213/81 ,  C07J9/00 ,  C07J17/00 ,  C07J31/00 ,  C07J41/00 ,  C07J43/00 ,  C07J51/00 ,  C07K5/06 ,  C07K5/062

Abstract: Bile acid derivatives of the formula I W-X-G in which G is a bile acid residue, W is an active substance portion of a medicament and X is a linker between bile acid residue and active substance portion, are outstandingly suitable for introducing active substances into the enterohepatic circulation. The compounds I are absorbed and enter the bloodstream. This makes it possible by utilising the natural reabsorption of the bile acids to improve the absorption of drugs which are absorbed with difficulty, if at all. W can be, for example, a peptide, an antibiotic, an antiviral substance, an anticancer agent, a liver protective, an antihyperlipidaemic, a diuretic, an agent to lower blood pressure, a renin inhibitor, a substance to treat cirrhosis of the liver or a substance for treating diabetes. G is a bile acid residue in the form of the free, natural or chemically modified acids, the esters and amides, the salt forms and forms derivatised on alcohol groups. X is a large number of intermediate members or else a bond.

公开(公告)号：DE4432708A1

公开(公告)日：1996-03-21

申请号：DE4432708

申请日：1994-09-14

Applicant: HOECHST AG

Inventor： WESS GUENTHER DR ,  ENHSEN ALFONS DR ,  KRAMER WERNER DR ,  BOCK KLAUS

IPC: A61K31/575 ,  A61K31/58 ,  A61K31/695 ,  A61P3/06 ,  C07J9/00 ,  C07J15/00 ,  C07J17/00 ,  C07J41/00 ,  C07J51/00 ,  C07J75/00 ,  C07F7/18

Abstract: Linker-modified bile acid derivs. of formula (I) are new. X = CH2OR, CH2NHR1, COOR2 or CH2N(CH2Ph)2; R = H, Sil, THP, trityl, acyl, COAr, CHO, COO-benzyl, CH2CH=CH2 or benzyl (opt. p-substd. by OMe); Sil = SiMe3, Si(Me)2- t-Bu or Si(Ph)2t-Bu; THP = tetrahydropyranyl; trityl = triphenylmethyl; t-Bu = tert. butyl; Ac = acetyl; acyl = 2-8C acyl; Ar = phenyl (opt. mono- to tri-substd. by 1-4C alkyl, OMe, F or Cl); R1 = H, acyl or COAr; R2 = H, alkali or alkaline earth metal, N(R4)4 or R5; R4 = independently H or 1-8C alkyl; R5 = alkyl or benzyl; R',R" = H, OH, O-THP, OAc, SiMe3, OSiMe2t-Bu, SiPh2t-Bu, OCH2Ar, OCH2CH=CH2, OCOCH2Ar, OCOAr or alkoxycarbonyl; Y = OH, 1-8C alkoxy, OCH2Ar, OAr, OM, ON(R6)4, OTHP, OCH2CH=CH2, NH2, NH(CH2)2SO3H, N(Me)(CH2)2SO3H, NHCH2COOH or N(Me)CH2COOH. Ph = phenyl; M = alkali metal; R6 = H or 1-8C alkyl; p = 2-49. R' is in the alpha or beta position; R" is only in the alpha position; and the OH in the 3 position is in the alpha or beta position.