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
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(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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1997-08-20
ATE152117T1
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1997-05-15
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US5646272A
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1997-07-08
EP0417725A2
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1991-03-20
KR910006319A
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1991-04-29
NO303450B1
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1998-07-13
DK0417725T3
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1997-11-03
IE903329A1
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1991-04-10
FI105155B
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2000-06-30
ES2100858T3
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1997-07-01
JP2642090B2
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1997-08-20
PT95299B
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1997-06-30
JPH0892277A
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1996-04-09
KR0166962B1
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1999-01-15
HU213395B
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1997-06-30
DE3930696A1
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1991-03-28
PT95299A
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1991-05-22
IL95668A
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1995-03-30
US5462933A
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1995-10-31
NO903999L
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1991-03-15
US5668126A
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1997-09-16
NO903999D0
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1990-09-13
EP0417725B1
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1997-04-23
AU637822B2
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1993-06-10
JP2568306B2
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1997-01-08
CA2025294A1
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1991-03-15
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1992-03-18
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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
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1991-06-30
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1993-05-26
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(en)
1991-06-26
HU905893D0
(en)
1991-03-28
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1996-04-09
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