Abstract

7-ketolithocholic acid (7-KCLA, 3α-hydroxy-7-oxo-5β-cholanic acid) and its pharmaceutically acceptable salts and glycine or taurine conjugates are useful for the prevention or treatment of gut dysbiosis, diseases and conditions associated with poor gut health, or in improving the health of the gut microbiome.

IPC Classes  ?

• A61K 31/575 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
• A61P 3/08 - Drugs for disorders of the metabolism for glucose homeostasis

Abstract

Compounds of formula (I): (I) wherein, R1, R2, R3, R4aand R4b are as defined herein are capable of restoring damaged mitochondria and are of use for treating neurodegenerative and neuromuscular diseases and disorders.

IPC Classes  ?

• A61P 25/00 - Drugs for disorders of the nervous system
• A61P 25/16 - Anti-Parkinson drugs
• A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
• C07J 9/00 - 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
• C07J 41/00 - Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
• C07J 43/00 - Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta[a]hydrophenanthrene skeleton

Abstract

Compounds of formula (I) wherein R1, R2and R3 are as defined herein are able to rescue dysfunctional mitochondria and are therefore of use in the treatment and prevention of neurodegenerative disorders as well as acute radiation syndrome and myalgic encephalomyelitis (ME, chronic fatigue syndrome) or post viral syndrome, including chronic symptoms arising from infection with SARS-CoV2 (long COVID).

IPC Classes  ?

• C07J 73/00 - Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms
• A61P 25/00 - Drugs for disorders of the nervous system
• A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
• A61P 31/12 - Antivirals
• A61P 31/14 - Antivirals for RNA viruses
• A61P 39/00 - General protective or antinoxious agents
• C07C 271/22 - Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by carboxyl groups

Abstract

7-ketolithocholic acid (7-KCLA, 3α-hydroxy-7-oxo-5β-cholanic acid) and its pharmaceutically acceptable salts and glycine or taurine conjugates are useful for the prevention or treatment of gut dysbiosis, diseases and conditions associated with poor gut health, or in improving the health of the gut microbiome.

IPC Classes  ?

• A61K 31/575 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• A61P 1/00 - Drugs for disorders of the alimentary tract or the digestive system

Abstract

Compounds of general formula (1): Compounds of general formula (1): Compounds of general formula (1): wherein R1, R2 and R3 are as defined herein; are of use in the treatment and prevention of neurodegenerative disorders including Alzheimer's disease and Parkinson's disease.

IPC Classes  ?

• C07J 9/00 - 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
• A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
• A61P 25/16 - Anti-Parkinson drugs
• C07J 31/00 - Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
• C07J 43/00 - Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta[a]hydrophenanthrene skeleton
• C07J 33/00 - Normal steroids having a sulfur-containing hetero ring spiro-condensed or not condensed with the cyclopenta[a]hydrophenanthrene skeleton

Abstract

The invention relates to compounds of general formula (I): 7 are as defined herein are selective agonists at the FXR receptor and are useful for the treatment or prevention of diseases and conditions including nonalcoholic steatohepatitis (NASH); primary biliary cirrhosis; primary sclerosing cholangitis; biliary atresia; cholestatic liver disease; hepatitis C infection; alcoholic liver disease; fibrosis; and liver damage arising from fibrosis.

IPC Classes  ?

• A61K 31/64 - Sulfonylureas, e.g. glibenclamide, tolbutamide, chlorpropamide
• A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
• A61K 31/575 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
• C07J 41/00 - Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring

Abstract

The present invention relates to compounds which are intermediates in the synthesis of bile acid derivatives with pharmacological activity. The invention relates to compounds of general formula (I): 6 and Y are as defined herein. The compounds are intermediates in the synthesis of synthetic bile acids which are useful in the treatment of conditions such as liver disease. In addition, the invention relates to a method of synthesizing these intermediates and a method of preparing obeticholic acid and obeticholic acid analogues from the compounds of the invention.

IPC Classes  ?

• C07J 43/00 - Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta[a]hydrophenanthrene skeleton
• C07J 9/00 - 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
• C07J 21/00 - Normal steroids containing carbon, hydrogen, halogen, or oxygen, having an oxygen-containing hetero ring spiro-condensed with the cyclopenta[a]hydrophenanthrene skeleton
• C07J 31/00 - Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
• C07J 41/00 - Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
• C07J 71/00 - Steroids in which the cyclopenta[a]hydrophenanthrene skeleton is condensed with a heterocyclic ring
• C07J 17/00 - Normal steroids containing carbon, hydrogen, halogen, or oxygen, having an oxygen-containing hetero ring not condensed with the cyclopenta[a]hydrophenanthrene skeleton
• C07J 33/00 - Normal steroids having a sulfur-containing hetero ring spiro-condensed or not condensed with the cyclopenta[a]hydrophenanthrene skeleton
• C07J 51/00 - Normal steroids with unmodified cyclopenta[a]hydrophenanthrene skeleton not provided for in groups
• C07J 13/00 - Normal steroids containing carbon, hydrogen, halogen, or oxygen, having a carbon-to-carbon double bond from or to position 17

Abstract

2-Fluorinated bile acid compounds of general formula (I) wherein at least one of R1and R2represents F and the other is chosen 3 from H and F and wherein R3 is as defined herein; are of use in the treatment and prevention of neurodegenerative disorders including Alzheimer's disease and Parkinson's disease.

IPC Classes  ?

• C07J 9/00 - 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
• C07J 41/00 - Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
• C07J 43/00 - Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta[a]hydrophenanthrene skeleton
• C07J 31/00 - Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
• A61K 31/575 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
• A61K 31/58 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
• A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
• C07J 51/00 - Normal steroids with unmodified cyclopenta[a]hydrophenanthrene skeleton not provided for in groups
• C07J 71/00 - Steroids in which the cyclopenta[a]hydrophenanthrene skeleton is condensed with a heterocyclic ring
• C07J 11/00 - Normal steroids containing carbon, hydrogen, halogen, or oxygen, not substituted in position 3

Abstract

Compounds of general formula (I): wherein R2a, R2b, R3a, R3b, R5, Y and R7 are as defined herein are selective agonists at the FXR receptor and are useful for the treatment or prevention of diseases and conditions including nonalcoholic steatohepatitis (NASH); primary biliary cirrhosis; primary sclerosing cholangitis; biliary atresia; cholestatic liver disease; hepatitis C infection; alcoholic liver disease; fibrosis; or liver damage arising from fibrosis.

IPC Classes  ?

• C07J 41/00 - Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
• A61K 31/575 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
• A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
• C07J 9/00 - 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
• C07J 11/00 - Normal steroids containing carbon, hydrogen, halogen, or oxygen, not substituted in position 3
• C07J 51/00 - Normal steroids with unmodified cyclopenta[a]hydrophenanthrene skeleton not provided for in groups
• C07J 71/00 - Steroids in which the cyclopenta[a]hydrophenanthrene skeleton is condensed with a heterocyclic ring

Abstract

5 are as defined herein, wherein the epoxidation is conducted using an oxidant and methyltrioxorhenium as a catalyst (MeReO3). The invention also relates to certain compounds per se. The compounds are intermediates in the synthesis of synthetic bile acids.

IPC Classes  ?

• C07J 71/00 - Steroids in which the cyclopenta[a]hydrophenanthrene skeleton is condensed with a heterocyclic ring
• C07J 9/00 - 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
• C07J 41/00 - Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
• C07J 43/00 - Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta[a]hydrophenanthrene skeleton
• C07J 31/00 - Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
• C07J 17/00 - Normal steroids containing carbon, hydrogen, halogen, or oxygen, having an oxygen-containing hetero ring not condensed with the cyclopenta[a]hydrophenanthrene skeleton
• C07J 13/00 - Normal steroids containing carbon, hydrogen, halogen, or oxygen, having a carbon-to-carbon double bond from or to position 17
• C07J 51/00 - Normal steroids with unmodified cyclopenta[a]hydrophenanthrene skeleton not provided for in groups

Abstract

The present invention relates to compounds which are intermediates in the synthesis of bile acid derivatives with pharmacological activity. The invention relates to compounds of general formula (I): 6 and Y are as defined herein. The compounds are intermediates in the synthesis of synthetic bile acids which are useful in the treatment of conditions such as liver disease. In addition, the invention relates to a method of synthesizing these intermediates and a method of preparing obeticholic acid and obeticholic acid analogues from the compounds of the invention.

IPC Classes  ?

• C07J 43/00 - Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta[a]hydrophenanthrene skeleton
• C07J 9/00 - 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
• C07J 21/00 - Normal steroids containing carbon, hydrogen, halogen, or oxygen, having an oxygen-containing hetero ring spiro-condensed with the cyclopenta[a]hydrophenanthrene skeleton
• C07J 31/00 - Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
• C07J 41/00 - Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
• C07J 51/00 - Normal steroids with unmodified cyclopenta[a]hydrophenanthrene skeleton not provided for in groups
• C07J 33/00 - Normal steroids having a sulfur-containing hetero ring spiro-condensed or not condensed with the cyclopenta[a]hydrophenanthrene skeleton
• C07J 13/00 - Normal steroids containing carbon, hydrogen, halogen, or oxygen, having a carbon-to-carbon double bond from or to position 17
• C07J 17/00 - Normal steroids containing carbon, hydrogen, halogen, or oxygen, having an oxygen-containing hetero ring not condensed with the cyclopenta[a]hydrophenanthrene skeleton
• C07J 71/00 - Steroids in which the cyclopenta[a]hydrophenanthrene skeleton is condensed with a heterocyclic ring

Abstract

Disclosed herein is a process for the preparation of a compound of formula (I) and related methods. The compounds of formula (I) are intermediates in the synthesis of synthetic bile acids and its analogues, and the compounds of formula (I) have pharmacological activity. Methods include the synthesizing of these intermediates, and methods of preparing obeticholic acid and obeticholic acid analogues from the prepared compounds.

IPC Classes  ?

• C07J 71/00 - Steroids in which the cyclopenta[a]hydrophenanthrene skeleton is condensed with a heterocyclic ring
• C07J 9/00 - 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

Abstract

5 are as defined herein. The compounds are intermediates in the synthesis of synthetic bile acid derivatives with pharmacological activity. The invention further provides methods related to the synthesizing of these intermediates, and methods of preparing obeticholic acid and obeticholic acid analogues from the compounds of the invention.

IPC Classes  ?

• C07J 9/00 - 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

Abstract

The invention relates to a process for preparing a compound of general formula (Ia): wherein R2, Y, R4 and R5 are as defined herein. The invention also relates to certain compounds per se. The compounds are intermediates in the synthesis of synthetic bile acids.

IPC Classes  ?

• C07J 9/00 - 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
• C07J 41/00 - Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
• C07J 71/00 - Steroids in which the cyclopenta[a]hydrophenanthrene skeleton is condensed with a heterocyclic ring
• C07J 13/00 - Normal steroids containing carbon, hydrogen, halogen, or oxygen, having a carbon-to-carbon double bond from or to position 17
• C07J 21/00 - Normal steroids containing carbon, hydrogen, halogen, or oxygen, having an oxygen-containing hetero ring spiro-condensed with the cyclopenta[a]hydrophenanthrene skeleton
• C07J 17/00 - Normal steroids containing carbon, hydrogen, halogen, or oxygen, having an oxygen-containing hetero ring not condensed with the cyclopenta[a]hydrophenanthrene skeleton
• C07J 31/00 - Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
• C07J 43/00 - Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta[a]hydrophenanthrene skeleton
• C07J 51/00 - Normal steroids with unmodified cyclopenta[a]hydrophenanthrene skeleton not provided for in groups

Abstract

The invention relates to compounds of general formula (I): wherein: R1, R2, R3, R4, R5, R6 and Y are as defined herein. The compounds are intermediates in the synthesis of synthetic bile acids which are useful in the treatment of conditions such as liver disease.

IPC Classes  ?

• C07J 71/00 - Steroids in which the cyclopenta[a]hydrophenanthrene skeleton is condensed with a heterocyclic ring
• C07J 9/00 - 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
• C07J 17/00 - Normal steroids containing carbon, hydrogen, halogen, or oxygen, having an oxygen-containing hetero ring not condensed with the cyclopenta[a]hydrophenanthrene skeleton
• C07J 33/00 - Normal steroids having a sulfur-containing hetero ring spiro-condensed or not condensed with the cyclopenta[a]hydrophenanthrene skeleton
• C07J 41/00 - Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
• C07J 43/00 - Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta[a]hydrophenanthrene skeleton
• C07J 51/00 - Normal steroids with unmodified cyclopenta[a]hydrophenanthrene skeleton not provided for in groups
• C07J 13/00 - Normal steroids containing carbon, hydrogen, halogen, or oxygen, having a carbon-to-carbon double bond from or to position 17
• C07J 21/00 - Normal steroids containing carbon, hydrogen, halogen, or oxygen, having an oxygen-containing hetero ring spiro-condensed with the cyclopenta[a]hydrophenanthrene skeleton
• C07J 31/00 - Normal steroids containing one or more sulfur atoms not belonging to a hetero ring

Abstract

The invention relates to a process for preparing a compound of general formula (la): wherein R2, Y, R4and R5are as defined herein, wherein the epoxidation is conducted using an oxidant and methyltrioxorhenium as a catalyst (MeReO3). The invention also relates to certain compounds per se.The compounds are intermediates in the synthesis of synthetic bile acids.

IPC Classes  ?

• C07J 9/00 - 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
• C07J 71/00 - Steroids in which the cyclopenta[a]hydrophenanthrene skeleton is condensed with a heterocyclic ring

Abstract

5 are as defined herein. The compounds are intermediates in the synthesis of synthetic bile acids with pharmacological activity. The invention futher provides intermediated in the systhesis of obeticholic acid and its analogues. The invention also provides methods related to the synthesizing of these intermediates and methods of preparing obeticholic acid and obeticholic acid analogues from the compound of the invention.

IPC Classes  ?

• C07J 9/00 - 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
• C07J 71/00 - Steroids in which the cyclopenta[a]hydrophenanthrene skeleton is condensed with a heterocyclic ring

Abstract

5 are as defined herein. The compounds are intermediates in the synthesis of synthetic bile acids.

IPC Classes  ?

• C07J 9/00 - 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
• C07J 71/00 - Steroids in which the cyclopenta[a]hydrophenanthrene skeleton is condensed with a heterocyclic ring

Abstract

The invention relates to compounds of formula (I): wherein R1, R2, Y, R4 and R5 are as defined herein. The compounds are intermediates in the synthesis of synthetic bile acids.

IPC Classes  ?

• C07J 9/00 - 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

Abstract

The invention relates to compounds of formula (I) wherein R1, R2, Y1, R4 and R5 are as defined herein. The compounds are intermediates in the synthesis of synthetic bile acids.

IPC Classes  ?

• C07J 9/00 - 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

Abstract

The invention relates to compounds of formula (I), wherein R1, R2, Y, R4 and R5b are as defined herein. The compounds are intermediates in the synthesis of synthetic bile acids.

IPC Classes  ?

• C07J 9/00 - 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

Abstract

The invention relates to compounds of formula (I), wherein R1, R2, Y, R4 and R5 are as defined herein. The compounds are intermediates in the synthesis of synthetic bile acids.

IPC Classes  ?

• C07J 9/00 - 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
• C07J 71/00 - Steroids in which the cyclopenta[a]hydrophenanthrene skeleton is condensed with a heterocyclic ring

Goods & Services

Chemicals for testing blood; blood culture media for scientific use; blood grouping reagents for scientific use. Blood components; blood substitutes; blood plasma; blood protein fractions; blood tonics; reagents for blood grouping for medical purposes; antigens. Custom manufacture of blood components, blood substitutes, blood plasma, blood protein fractions, blood tonics, reagents for blood grouping for medical purposes and antigens.

Goods & Services

Chemicals for testing blood; blood culture media for scientific use; blood grouping reagents for scientific use. Blood components; blood substitutes; blood plasma; blood protein fractions; blood tonics; reagents for blood grouping for medical purposes; antigens. Custom manufacture of blood components, blood substitutes, blood plasma, blood protein fractions, blood tonics, reagents for blood grouping for medical purposes and antigens.

Abstract

Compounds of general formula (I): wherein at least one of R1and R2 represents F and the other is chosen from H and F and wherein R3 is as defined herein; are of use in the treatment and prevention of neurodegenerative disorders including Alzheimer's disease and Parkinson's disease.

IPC Classes  ?

• A61K 31/575 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
• A61K 31/58 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
• A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
• C07J 9/00 - 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
• C07J 11/00 - Normal steroids containing carbon, hydrogen, halogen, or oxygen, not substituted in position 3
• C07J 31/00 - Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
• C07J 41/00 - Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
• C07J 43/00 - Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta[a]hydrophenanthrene skeleton
• C07J 51/00 - Normal steroids with unmodified cyclopenta[a]hydrophenanthrene skeleton not provided for in groups
• C07J 71/00 - Steroids in which the cyclopenta[a]hydrophenanthrene skeleton is condensed with a heterocyclic ring

Abstract

The invention relates to compounds of formula (I): wherein R1, R2, Y, R4 and R5 are as defined herein. The compounds are intermediates in the synthesis of synthetic bile acids.

IPC Classes  ?

• C07J 9/00 - 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
• C07J 75/00 - Processes for the preparation of steroids, in general

Abstract

The invention relates to compounds of general formula (I): wherein: R1,R2, R3, R4, R5, R6 and Y are as defined herein. The compounds are intermediates in the synthesis of synthetic bile acids which are useful in the treatment of conditions such as liver disease.

IPC Classes  ?

• C07J 9/00 - 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
• C07J 13/00 - Normal steroids containing carbon, hydrogen, halogen, or oxygen, having a carbon-to-carbon double bond from or to position 17
• C07J 17/00 - Normal steroids containing carbon, hydrogen, halogen, or oxygen, having an oxygen-containing hetero ring not condensed with the cyclopenta[a]hydrophenanthrene skeleton
• C07J 21/00 - Normal steroids containing carbon, hydrogen, halogen, or oxygen, having an oxygen-containing hetero ring spiro-condensed with the cyclopenta[a]hydrophenanthrene skeleton
• C07J 31/00 - Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
• C07J 33/00 - Normal steroids having a sulfur-containing hetero ring spiro-condensed or not condensed with the cyclopenta[a]hydrophenanthrene skeleton
• C07J 41/00 - Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
• C07J 43/00 - Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta[a]hydrophenanthrene skeleton
• C07J 51/00 - Normal steroids with unmodified cyclopenta[a]hydrophenanthrene skeleton not provided for in groups
• C07J 71/00 - Steroids in which the cyclopenta[a]hydrophenanthrene skeleton is condensed with a heterocyclic ring

Abstract

The invention relates to a process for preparing a compound of general formula (la): wherein R2, Y, R4and R5are as defined herein, wherein the epoxidation is conducted using an oxidant and methyltrioxorhenium as a catalyst (MeReO3). The invention also relates to certain compounds per se.The compounds are intermediates in the synthesis of synthetic bile acids.

IPC Classes  ?

• C07J 9/00 - 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
• C07J 71/00 - Steroids in which the cyclopenta[a]hydrophenanthrene skeleton is condensed with a heterocyclic ring

Abstract

The invention relates to a process for preparing a compound of general formula (Ia): wherein R2, Y, R4 and R5 are as defined herein. The invention also relates to certain compounds per se. The compounds are intermediates in the synthesis of synthetic bile acids.

IPC Classes  ?

• C07J 9/00 - 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
• C07J 13/00 - Normal steroids containing carbon, hydrogen, halogen, or oxygen, having a carbon-to-carbon double bond from or to position 17
• C07J 17/00 - Normal steroids containing carbon, hydrogen, halogen, or oxygen, having an oxygen-containing hetero ring not condensed with the cyclopenta[a]hydrophenanthrene skeleton
• C07J 21/00 - Normal steroids containing carbon, hydrogen, halogen, or oxygen, having an oxygen-containing hetero ring spiro-condensed with the cyclopenta[a]hydrophenanthrene skeleton
• C07J 31/00 - Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
• C07J 41/00 - Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
• C07J 43/00 - Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta[a]hydrophenanthrene skeleton
• C07J 51/00 - Normal steroids with unmodified cyclopenta[a]hydrophenanthrene skeleton not provided for in groups
• C07J 71/00 - Steroids in which the cyclopenta[a]hydrophenanthrene skeleton is condensed with a heterocyclic ring