AU6244190A

AU6244190A – Bile acid derivatives, processes for their preparation, and use as pharmaceuticals
– Google Patents

AU6244190A – Bile acid derivatives, processes for their preparation, and use as pharmaceuticals
– Google Patents
Bile acid derivatives, processes for their preparation, and use as pharmaceuticals

Info

Publication number
AU6244190A

AU6244190A
AU62441/90A
AU6244190A
AU6244190A
AU 6244190 A
AU6244190 A
AU 6244190A
AU 62441/90 A
AU62441/90 A
AU 62441/90A
AU 6244190 A
AU6244190 A
AU 6244190A
AU 6244190 A
AU6244190 A
AU 6244190A
Authority
AU
Australia
Prior art keywords
bile acid
substance
acid residue
acid derivatives
absorbed
Prior art date
1989-09-14
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)

Granted

Application number
AU62441/90A
Other versions

AU637822B2
(en

Inventor
Werner Kramer
Gunther Wess
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)

Hoechst AG

Original Assignee
Hoechst AG
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
1989-09-14
Filing date
1990-09-13
Publication date
1991-03-21

1990-09-13
Application filed by Hoechst AG
filed
Critical
Hoechst AG

1991-03-21
Publication of AU6244190A
publication
Critical
patent/AU6244190A/en

1993-06-10
Application granted
granted
Critical

1993-06-10
Publication of AU637822B2
publication
Critical
patent/AU637822B2/en

2010-09-13
Anticipated expiration
legal-status
Critical

Status
Expired
legal-status
Critical
Current

Links

Espacenet

Global Dossier

Discuss

Classifications

C—CHEMISTRY; METALLURGY

C07—ORGANIC CHEMISTRY

C07D—HETEROCYCLIC COMPOUNDS

C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members

C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members

C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom

C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms

C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals

C07D213/81—Amides; Imides

C—CHEMISTRY; METALLURGY

C07—ORGANIC CHEMISTRY

C07J—STEROIDS

C07J9/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane

A—HUMAN NECESSITIES

A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE

A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

A61P1/00—Drugs for disorders of the alimentary tract or the digestive system

A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics

A—HUMAN NECESSITIES

A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE

A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

A61P3/00—Drugs for disorders of the metabolism

A61P3/06—Antihyperlipidemics

A—HUMAN NECESSITIES

A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE

A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

C—CHEMISTRY; METALLURGY

C07—ORGANIC CHEMISTRY

C07D—HETEROCYCLIC COMPOUNDS

C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members

C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members

C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom

C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms

C07D213/26—Radicals substituted by halogen atoms or nitro radicals

C—CHEMISTRY; METALLURGY

C07—ORGANIC CHEMISTRY

C07D—HETEROCYCLIC COMPOUNDS

C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members

C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members

C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom

C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms

C07D213/54—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals

C07D213/56—Amides

C—CHEMISTRY; METALLURGY

C07—ORGANIC CHEMISTRY

C07J—STEROIDS

C07J17/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, having an oxygen-containing hetero ring not condensed with the cyclopenta(a)hydrophenanthrene skeleton

C—CHEMISTRY; METALLURGY

C07—ORGANIC CHEMISTRY

C07J—STEROIDS

C07J31/00—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring

C07J31/006—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring not covered by C07J31/003

C—CHEMISTRY; METALLURGY

C07—ORGANIC CHEMISTRY

C07J—STEROIDS

C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring

C07J41/0005—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring the nitrogen atom being directly linked to the cyclopenta(a)hydro phenanthrene skeleton

C07J41/0011—Unsubstituted amino radicals

C—CHEMISTRY; METALLURGY

C07—ORGANIC CHEMISTRY

C07J—STEROIDS

C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring

C07J41/0005—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring the nitrogen atom being directly linked to the cyclopenta(a)hydro phenanthrene skeleton

C07J41/0027—Azides

C—CHEMISTRY; METALLURGY

C07—ORGANIC CHEMISTRY

C07J—STEROIDS

C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring

C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005

C07J41/0055—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the 17-beta position being substituted by an uninterrupted chain of at least three carbon atoms which may or may not be branched, e.g. cholane or cholestane derivatives, optionally cyclised, e.g. 17-beta-phenyl or 17-beta-furyl derivatives

C—CHEMISTRY; METALLURGY

C07—ORGANIC CHEMISTRY

C07J—STEROIDS

C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring

C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005

C07J41/0055—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the 17-beta position being substituted by an uninterrupted chain of at least three carbon atoms which may or may not be branched, e.g. cholane or cholestane derivatives, optionally cyclised, e.g. 17-beta-phenyl or 17-beta-furyl derivatives

C07J41/0061—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the 17-beta position being substituted by an uninterrupted chain of at least three carbon atoms which may or may not be branched, e.g. cholane or cholestane derivatives, optionally cyclised, e.g. 17-beta-phenyl or 17-beta-furyl derivatives one of the carbon atoms being part of an amide group

C—CHEMISTRY; METALLURGY

C07—ORGANIC CHEMISTRY

C07J—STEROIDS

C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring

C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005

C07J41/0088—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 containing unsubstituted amino radicals

C—CHEMISTRY; METALLURGY

C07—ORGANIC CHEMISTRY

C07J—STEROIDS

C07J43/00—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton

C07J43/003—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed

C—CHEMISTRY; METALLURGY

C07—ORGANIC CHEMISTRY

C07J—STEROIDS

C07J51/00—Normal steroids with unmodified cyclopenta(a)hydrophenanthrene skeleton not provided for in groups C07J1/00 – C07J43/00

C—CHEMISTRY; METALLURGY

C07—ORGANIC CHEMISTRY

C07J—STEROIDS

C07J9/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane

C07J9/005—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane containing a carboxylic function directly attached or attached by a chain containing only carbon atoms to the cyclopenta[a]hydrophenanthrene skeleton

C—CHEMISTRY; METALLURGY

C07—ORGANIC CHEMISTRY

C07K—PEPTIDES

C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof

C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links

C07K5/06—Dipeptides

C07K5/06008—Dipeptides with the first amino acid being neutral

C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic

C07K5/06026—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala

A—HUMAN NECESSITIES

A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE

A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES

A61K38/00—Medicinal preparations containing peptides

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.

AU62441/90A
1989-09-14
1990-09-13
Bile acid derivatives, processes for their preparation, and use as pharmaceuticals

Expired

AU637822B2
(en)

Applications Claiming Priority (2)

Application Number
Priority Date
Filing Date
Title

DE3930696A

DE3930696A1
(en)

1989-09-14
1989-09-14

GALLENSAEUREDERIVATE, METHOD FOR THE PRODUCTION THEREOF, USE AS MEDICAMENT

DE3930696

1989-09-14

Publications (2)

Publication Number
Publication Date

AU6244190A
true

AU6244190A
(en)

1991-03-21

AU637822B2

AU637822B2
(en)

1993-06-10

Family
ID=6389405
Family Applications (1)

Application Number
Title
Priority Date
Filing Date

AU62441/90A
Expired

AU637822B2
(en)

1989-09-14
1990-09-13
Bile acid derivatives, processes for their preparation, and use as pharmaceuticals

Country Status (21)

Country
Link

US
(3)

US5462933A
(en)

EP
(1)

EP0417725B1
(en)

JP
(3)

JP2568306B2
(en)

KR
(1)

KR0166962B1
(en)

AT
(1)

ATE152117T1
(en)

AU
(1)

AU637822B2
(en)

CA
(1)

CA2025294C
(en)

CY
(1)

CY2112B1
(en)

DE
(2)

DE3930696A1
(en)

DK
(1)

DK0417725T3
(en)

ES
(1)

ES2100858T3
(en)

FI
(1)

FI105155B
(en)

GR
(1)

GR3024095T3
(en)

HU
(1)

HU213395B
(en)

IE
(1)

IE903329A1
(en)

IL
(1)

IL95668A
(en)

NO
(1)

NO303450B1
(en)

NZ
(1)

NZ235285A
(en)

PT
(1)

PT95299B
(en)

TW
(1)

TW199097B
(en)

ZA
(1)

ZA907300B
(en)

Cited By (1)

* Cited by examiner, † Cited by third party

Publication number
Priority date
Publication date
Assignee
Title

AU665799B2
(en)

*

1991-12-13
1996-01-18
Trustees Of Princeton University, The
Glycosylated steroid acid derivatives for transport across biological membranes

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1989-09-14
1991-03-28
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GALLENSAEUREDERIVATE, METHOD FOR THE PRODUCTION THEREOF, USE AS MEDICAMENT

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Trustees Of Princeton University, The
Glycosylated steroid acid derivatives for transport across biological membranes

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(en)

1997-08-20

ATE152117T1
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1997-05-15

GR3024095T3
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1997-10-31

US5646272A
(en)

1997-07-08

EP0417725A2
(en)

1991-03-20

KR910006319A
(en)

1991-04-29

NO303450B1
(en)

1998-07-13

DK0417725T3
(en)

1997-11-03

IE903329A1
(en)

1991-04-10

FI105155B
(en)

2000-06-30

ES2100858T3
(en)

1997-07-01

JP2642090B2
(en)

1997-08-20

PT95299B
(en)

1997-06-30

JPH0892277A
(en)

1996-04-09

KR0166962B1
(en)

1999-01-15

HU213395B
(en)

1997-06-30

DE3930696A1
(en)

1991-03-28

PT95299A
(en)

1991-05-22

IL95668A
(en)

1995-03-30

US5462933A
(en)

1995-10-31

NO903999L
(en)

1991-03-15

US5668126A
(en)

1997-09-16

NO903999D0
(en)

1990-09-13

EP0417725B1
(en)

1997-04-23

AU637822B2
(en)

1993-06-10

JP2568306B2
(en)

1997-01-08

CA2025294A1
(en)

1991-03-15

EP0417725A3
(en)

1992-03-18

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(en)

1990-09-12

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2001-11-27

HUT56115A
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1991-07-29

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1991-05-09

IL95668A0
(en)

1991-06-30

NZ235285A
(en)

1993-05-26

ZA907300B
(en)

1991-06-26

HU905893D0
(en)

1991-03-28

JPH0892276A
(en)

1996-04-09

CY2112B1
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1993-02-01

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1997-05-28

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