US 2011/0218204 A1 · PHARMACEUTICALLY ACCEPTABLE SALTS OF NOVEL BETULINIC ACID DERIVATIVES

Abstract

The present invention relates to certain novel salts of Betulinic acid derivatives, to process for preparing such compounds, to use the compounds in treating diseases or disorders mediated by HIV infection, to methods for their therapeutic use and to pharmaceutical compositions containing them.

Claims26

Dependent claims

A salt of a compound of formula (I):

Wherein,
R is OH,
W is
Salt is an arginine, amino guanidine, choline, dicyclohexylamine, diethanolamine, dimethyl piperazine, lithium, lysine, magnesium, N-methyl glucamine, N-octyl glucamine, piperazine, phenyl glycine methyl ester, phenyl glycinol, potassium, sodium, Trizma base primary standard buffer, or calcium, stereoisomers, including enantiomers, diastereomers, racemates, or mixtures thereof.

1 more element

A salt of a compound selected from the group consisting of:

Arginine salt of 4-((1R,3aR,5aR,5bR,9S,11aR)-3a-((1R,3S)-2,2-dimethyl-3-(piperidine-1-carbonyl)cyclobutylcarbamoyl)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yloxy)-2,2-dimethyl-4-oxobutanoic acid (Compound 1),
Amino guanidine salt of 4-((1R,3aR,5aR,5bR,9S,11aR)-3a-((1R,3S)-2,2-dimethyl-3-(piperidine-1-carbonyl)cyclobutylcarbamoyl)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yloxy)-2,2-dimethyl-4-oxobutanoic acid (Compound 2),
Calcium salt of 4-((1R,3aR,5aR,5bR,9S,11aR)-3a-((1R,3S)-2,2-dimethyl-3-(piperidine-1-carbonyl)cyclobutylcarbamoyl)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yloxy)-2,2-dimethyl-4-oxobutanoic acid (Compound 3),
Choline salt of 4-((1R,3aR,5aR,5bR,9S,11aR)-3a-((1R,3S)-2,2-dimethyl-3-(piperidine-1-carbonyl)cyclobutylcarbamoyl)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yloxy)-2,2-dimethyl-4-oxobutanoic acid (Compound 4),
Dicyclohexylamine salt of 4-((1R,3aR,5aR,5bR,9S,11aR)-3a-((1R,3S)-2,2-dimethyl-3-(piperidine-1-carbonyl)cyclobutylcarbamoyl)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yloxy)-2,2-dimethyl-4-oxobutanoic acid (Compound 5),
Diethanolamine salt of 4-((1R,3aR,5aR,5bR,9S,11aR)-3a-((1R,3S)-2,2-dimethyl-3-(piperidine-1-carbonyl)cyclobutylcarbamoyl)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yloxy)-2,2-dimethyl-4-oxobutanoic acid (Compound 6),
2,6-dimethyl Piperazine salt of 4-((1R,3aR,5aR,5bR,9S,11aR)-3a-((1R,3S)-2,2-dimethyl-3-(piperidine-1-carbonyl)cyclobutylcarbamoyl)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yloxy)-2,2-dimethyl-4-oxobutanoic acid (Compound 7),
Lithium salt of 4-((1R,3aR,5aR,5bR,9S,11aR)-3a-((1R,3S)-2,2-dimethyl-3-(piperidine-1-carbonyl)cyclobutylcarbamoyl)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yloxy)-2,2-dimethyl-4-oxobutanoic acid (Compound 8),
Lysine salt of 4-((1R,3aR,5aR,5bR,9S,11aR)-3a-((1R,3S)-2,2-dimethyl-3-(piperidine-1-carbonyl)cyclobutylcarbamoyl)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yloxy)-2,2-dimethyl-4-oxobutanoic acid (Compound 9),
Magnesium salt of 4-((1R,3aR,5aR,5bR,9S,11aR)-3a-((1R,3S)-2,2-dimethyl-3-(piperidine-1-carbonyl)cyclobutylcarbamoyl)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yloxy)-2,2-dimethyl-4-oxobutanoic acid (Compound 10),
N-methyl Glucamine salt of 4-((1R,3aR,5aR,5bR,9S,11aR)-3a-((1R,3S)-2,2-dimethyl-3-(piperidine-1-carbonyl)cyclobutylcarbamoyl)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yloxy)-2,2-dimethyl-4-oxobutanoic acid (Compound 11),
N-octyl Glucamine salt of 4-((1R,3aR,5aR,5bR,9S,11aR)-3a-((1R,3S)-2,2-dimethyl-3-(piperidine-1-carbonyl)cyclobutylcarbamoyl)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yloxy)-2,2-dimethyl-4-oxobutanoic acid (Compound 12),
Piperazine salt of 4-((1R,3aR,5aR,5bR,9S,11aR)-3a-((1R,3S)-2,2-dimethyl-3-(piperidine-1-carbonyl)cyclobutylcarbamoyl)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yloxy)-2,2-dimethyl-4-oxobutanoic acid (Compound 13),
Phenyl glycine methyl ester salt of 4-((1R,3aR,5aR,5bR,9S,11aR)-3a-((1R,3S)-2,2-dimethyl-3-(piperidine-1-carbonyl)cyclobutylcarbamoyl)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)icosahydro-1H- cyclopenta[a]chrysen-9-yloxy)-2,2-dimethyl-4-oxobutanoic acid (Compound 14),
Phenyl glycinol salt of 4-((1R,3aR,5aR,5bR,9S,11aR)-3a-((1R,3S)-2,2-dimethyl-3-(piperidine-1- carbonyl)cyclobutylcarbamoyl)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yloxy)-2,2-dimethyl-4-oxobutanoic acid (Compound 15),
Potassium salt of 4-((1R,3aR,5aR,5bR,9S,11aR)-3a-((1R,3S)-2,2-dimethyl-3-(piperidine-1-carbonyl)cyclobutylcarbamoyl)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yloxy)-2,2-dimethyl-4-oxobutanoic acid (Compound 16),
Sodium salt of 4-((1R,3aR,5aR,5bR,9S,11aR)-3a-((1R,3S)-2,2-dimethyl-3-(piperidine-1-carbonyl)cyclobutylcarbamoyl)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yloxy)-2,2-dimethyl-4-oxobutanoic acid (Compound 17),
Tris(hydroxymethyl)amino methane salt of 4-((1R,3aR,5aR,5bR,9S,11aR)-3a-((1R,3S)-2,2-dimethyl-3-(piperidine-1-carbonyl)cyclobutylcarbamoyl)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yloxy)-2,2-dimethyl-4-oxobutanoic acid (Compound 18),
Sodium salt of 4-((1R,3aS,5aS,7aR,9S,11aR,11bS,13aR)-3a-((1S,3S)-2,2-dimethyl-3-(pyrrolidine-1-carbonyl)cyclobutylcarbamoyl)-5a,8,8,11a,13a-pentamethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yloxy)-2,2-dimethyl-4-oxobutanoic acid (Compound 19),
Potassium salt of 4-((1R,3aS,5aS,7aR,9S,11aR,11bS,13aR)-3a-((1S,3S)-2,2-dimethyl-3-(pyrrolidine-1-carbonyl)cyclobutylcarbamoyl)-5a,8,8,11a,13a-pentamethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yloxy)-2,2-dimethyl-4-oxobutanoic acid (Compound 20),
N-methyl Glucamine salt of 4-((1R,3aS,5aS,7aR,9S,11aR,11bS,13aR)-3a-((1S,3S)-2,2-dimethyl-3-(pyrrolidine-1-carbonyl)cyclobutylcarbamoyl)-5a,8,8,11a,13a-pentamethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yloxy)-2,2-dimethyl-4-oxobutanoic acid (Compound 21),
Arginine salt of (1R,5bS,9S,11aR)-9-((1R,3S)-3-carboxy-2,2-dimethylcyclobutanecarbonyloxy)-5b,8,8,11a-tetramethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysene-3a-carboxylic acid (Compound 22),
Choline hydroxide salt of (1R,5bS,9S,11aR)-9-((1R,3S)-3-carboxy-2,2-dimethylcyclobutanecarbonyloxy)-5b,8,8,11a-tetramethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysene-3a-carboxylic acid (Compound 23),
Diethanolamine salt of (1R,5bS,9S,11aR)-9-((1R,3S)-3-carboxy-2,2-dimethylcyclobutanecarbonyloxy)-5b,8,8,11a-tetramethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysene-3a-carboxylic acid (Compound 24),
Bis-N-methyl glucamine salt of (1R,5bS,9S,11aR)-9-((1R,3S)-3-carboxy-2,2-dimethylcyclobutanecarbonyloxy)-5b,8,8,11a-tetramethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysene-3 a-carboxylic acid (Compound 25),
Dipotassium salt of (1R,5bS,9S,11aR)-9-((1R,3S)-3-carboxy-2,2-dimethylcyclobutanecarbonyloxy)-5b,8,8,11a-tetramethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysene-3 a-carboxylic acid (Compound 26),
Disodium salt of (1R,5bS,9S,11aR)-9-((1R,3S)-3-carboxy-2,2-dimethylcyclobutanecarbonyloxy)-5b,8,8,11a-tetramethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysene-3a-carboxylic acid (Compound 27),
and pharmaceutically acceptable solvates, including hydrates and prodrugs, thereof.

25 more elements

Dependencies are inferred from the claim text.

Facts

Application

12/987,228Filed 10 Jan 2011

Priority

IN 1670/CHE/200914 Jul 2009

Published

8 Sep 2011

Term ends

Not estimatedThe source records don’t support an estimate.

Classification13 codes

C07J 63/008
Steroids in which the cyclopentahydrophenanthrene skeleton has been modified by expansion of only one ring by one or two atoms: expansion of ring…
A61K 31/215
Esters, e.g. nitroglycerine, selenocyanates: of carboxylic acids
A61K 31/40
Having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins: having five-membered rings with one nitrogen as the only ring hetero atom,…
A61K 31/4453
Non condensed piperidines, e.g. piperocaine: only substituted in position 1, e.g. propipocaine, diperodon

Family

Application61/251,933Us provisional application · filed 15 Oct 2009

Application12/829,483Continuation in part · filed 2 Jul 2010

Application12/987,228Continuation in part

US 2011/0015196 A1Published application

US 8,802,727 B2Related patent

US 9,067,966 B2Related patent

US 2011/0218204 A1This patent

From the US filing history. Foreign family members aren’t listed.

Abstract

Claims26

Dependent claims

A salt of a compound of formula (I):

Wherein,
R is OH,
W is
Salt is an arginine, amino guanidine, choline, dicyclohexylamine, diethanolamine, dimethyl piperazine, lithium, lysine, magnesium, N-methyl glucamine, N-octyl glucamine, piperazine, phenyl glycine methyl ester, phenyl glycinol, potassium, sodium, Trizma base primary standard buffer, or calcium, stereoisomers, including enantiomers, diastereomers, racemates, or mixtures thereof.

1 more element

A salt of a compound selected from the group consisting of:

Arginine salt of 4-((1R,3aR,5aR,5bR,9S,11aR)-3a-((1R,3S)-2,2-dimethyl-3-(piperidine-1-carbonyl)cyclobutylcarbamoyl)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yloxy)-2,2-dimethyl-4-oxobutanoic acid (Compound 1),
Amino guanidine salt of 4-((1R,3aR,5aR,5bR,9S,11aR)-3a-((1R,3S)-2,2-dimethyl-3-(piperidine-1-carbonyl)cyclobutylcarbamoyl)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yloxy)-2,2-dimethyl-4-oxobutanoic acid (Compound 2),
Calcium salt of 4-((1R,3aR,5aR,5bR,9S,11aR)-3a-((1R,3S)-2,2-dimethyl-3-(piperidine-1-carbonyl)cyclobutylcarbamoyl)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yloxy)-2,2-dimethyl-4-oxobutanoic acid (Compound 3),
Choline salt of 4-((1R,3aR,5aR,5bR,9S,11aR)-3a-((1R,3S)-2,2-dimethyl-3-(piperidine-1-carbonyl)cyclobutylcarbamoyl)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yloxy)-2,2-dimethyl-4-oxobutanoic acid (Compound 4),
Dicyclohexylamine salt of 4-((1R,3aR,5aR,5bR,9S,11aR)-3a-((1R,3S)-2,2-dimethyl-3-(piperidine-1-carbonyl)cyclobutylcarbamoyl)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yloxy)-2,2-dimethyl-4-oxobutanoic acid (Compound 5),
Diethanolamine salt of 4-((1R,3aR,5aR,5bR,9S,11aR)-3a-((1R,3S)-2,2-dimethyl-3-(piperidine-1-carbonyl)cyclobutylcarbamoyl)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yloxy)-2,2-dimethyl-4-oxobutanoic acid (Compound 6),
2,6-dimethyl Piperazine salt of 4-((1R,3aR,5aR,5bR,9S,11aR)-3a-((1R,3S)-2,2-dimethyl-3-(piperidine-1-carbonyl)cyclobutylcarbamoyl)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yloxy)-2,2-dimethyl-4-oxobutanoic acid (Compound 7),
Lithium salt of 4-((1R,3aR,5aR,5bR,9S,11aR)-3a-((1R,3S)-2,2-dimethyl-3-(piperidine-1-carbonyl)cyclobutylcarbamoyl)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yloxy)-2,2-dimethyl-4-oxobutanoic acid (Compound 8),
Lysine salt of 4-((1R,3aR,5aR,5bR,9S,11aR)-3a-((1R,3S)-2,2-dimethyl-3-(piperidine-1-carbonyl)cyclobutylcarbamoyl)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yloxy)-2,2-dimethyl-4-oxobutanoic acid (Compound 9),
Magnesium salt of 4-((1R,3aR,5aR,5bR,9S,11aR)-3a-((1R,3S)-2,2-dimethyl-3-(piperidine-1-carbonyl)cyclobutylcarbamoyl)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yloxy)-2,2-dimethyl-4-oxobutanoic acid (Compound 10),
N-methyl Glucamine salt of 4-((1R,3aR,5aR,5bR,9S,11aR)-3a-((1R,3S)-2,2-dimethyl-3-(piperidine-1-carbonyl)cyclobutylcarbamoyl)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yloxy)-2,2-dimethyl-4-oxobutanoic acid (Compound 11),
N-octyl Glucamine salt of 4-((1R,3aR,5aR,5bR,9S,11aR)-3a-((1R,3S)-2,2-dimethyl-3-(piperidine-1-carbonyl)cyclobutylcarbamoyl)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yloxy)-2,2-dimethyl-4-oxobutanoic acid (Compound 12),
Piperazine salt of 4-((1R,3aR,5aR,5bR,9S,11aR)-3a-((1R,3S)-2,2-dimethyl-3-(piperidine-1-carbonyl)cyclobutylcarbamoyl)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yloxy)-2,2-dimethyl-4-oxobutanoic acid (Compound 13),
Phenyl glycine methyl ester salt of 4-((1R,3aR,5aR,5bR,9S,11aR)-3a-((1R,3S)-2,2-dimethyl-3-(piperidine-1-carbonyl)cyclobutylcarbamoyl)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)icosahydro-1H- cyclopenta[a]chrysen-9-yloxy)-2,2-dimethyl-4-oxobutanoic acid (Compound 14),
Phenyl glycinol salt of 4-((1R,3aR,5aR,5bR,9S,11aR)-3a-((1R,3S)-2,2-dimethyl-3-(piperidine-1- carbonyl)cyclobutylcarbamoyl)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yloxy)-2,2-dimethyl-4-oxobutanoic acid (Compound 15),
Potassium salt of 4-((1R,3aR,5aR,5bR,9S,11aR)-3a-((1R,3S)-2,2-dimethyl-3-(piperidine-1-carbonyl)cyclobutylcarbamoyl)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yloxy)-2,2-dimethyl-4-oxobutanoic acid (Compound 16),
Sodium salt of 4-((1R,3aR,5aR,5bR,9S,11aR)-3a-((1R,3S)-2,2-dimethyl-3-(piperidine-1-carbonyl)cyclobutylcarbamoyl)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yloxy)-2,2-dimethyl-4-oxobutanoic acid (Compound 17),
Tris(hydroxymethyl)amino methane salt of 4-((1R,3aR,5aR,5bR,9S,11aR)-3a-((1R,3S)-2,2-dimethyl-3-(piperidine-1-carbonyl)cyclobutylcarbamoyl)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yloxy)-2,2-dimethyl-4-oxobutanoic acid (Compound 18),
Sodium salt of 4-((1R,3aS,5aS,7aR,9S,11aR,11bS,13aR)-3a-((1S,3S)-2,2-dimethyl-3-(pyrrolidine-1-carbonyl)cyclobutylcarbamoyl)-5a,8,8,11a,13a-pentamethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yloxy)-2,2-dimethyl-4-oxobutanoic acid (Compound 19),
Potassium salt of 4-((1R,3aS,5aS,7aR,9S,11aR,11bS,13aR)-3a-((1S,3S)-2,2-dimethyl-3-(pyrrolidine-1-carbonyl)cyclobutylcarbamoyl)-5a,8,8,11a,13a-pentamethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yloxy)-2,2-dimethyl-4-oxobutanoic acid (Compound 20),
N-methyl Glucamine salt of 4-((1R,3aS,5aS,7aR,9S,11aR,11bS,13aR)-3a-((1S,3S)-2,2-dimethyl-3-(pyrrolidine-1-carbonyl)cyclobutylcarbamoyl)-5a,8,8,11a,13a-pentamethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-yloxy)-2,2-dimethyl-4-oxobutanoic acid (Compound 21),
Arginine salt of (1R,5bS,9S,11aR)-9-((1R,3S)-3-carboxy-2,2-dimethylcyclobutanecarbonyloxy)-5b,8,8,11a-tetramethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysene-3a-carboxylic acid (Compound 22),
Choline hydroxide salt of (1R,5bS,9S,11aR)-9-((1R,3S)-3-carboxy-2,2-dimethylcyclobutanecarbonyloxy)-5b,8,8,11a-tetramethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysene-3a-carboxylic acid (Compound 23),
Diethanolamine salt of (1R,5bS,9S,11aR)-9-((1R,3S)-3-carboxy-2,2-dimethylcyclobutanecarbonyloxy)-5b,8,8,11a-tetramethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysene-3a-carboxylic acid (Compound 24),
Bis-N-methyl glucamine salt of (1R,5bS,9S,11aR)-9-((1R,3S)-3-carboxy-2,2-dimethylcyclobutanecarbonyloxy)-5b,8,8,11a-tetramethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysene-3 a-carboxylic acid (Compound 25),
Dipotassium salt of (1R,5bS,9S,11aR)-9-((1R,3S)-3-carboxy-2,2-dimethylcyclobutanecarbonyloxy)-5b,8,8,11a-tetramethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysene-3 a-carboxylic acid (Compound 26),
Disodium salt of (1R,5bS,9S,11aR)-9-((1R,3S)-3-carboxy-2,2-dimethylcyclobutanecarbonyloxy)-5b,8,8,11a-tetramethyl-1-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysene-3a-carboxylic acid (Compound 27),
and pharmaceutically acceptable solvates, including hydrates and prodrugs, thereof.

25 more elements

Dependencies are inferred from the claim text.

Facts

Application

12/987,228Filed 10 Jan 2011

Priority

IN 1670/CHE/200914 Jul 2009

Published

8 Sep 2011

Term ends

Not estimatedThe source records don’t support an estimate.

Classification13 codes

C07J 63/008
Steroids in which the cyclopentahydrophenanthrene skeleton has been modified by expansion of only one ring by one or two atoms: expansion of ring…
A61K 31/215
Esters, e.g. nitroglycerine, selenocyanates: of carboxylic acids
A61K 31/40
Having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins: having five-membered rings with one nitrogen as the only ring hetero atom,…
A61K 31/4453
Non condensed piperidines, e.g. piperocaine: only substituted in position 1, e.g. propipocaine, diperodon

Family

Application61/251,933Us provisional application · filed 15 Oct 2009

Application12/829,483Continuation in part · filed 2 Jul 2010

Application12/987,228Continuation in part

US 2011/0015196 A1Published application

US 8,802,727 B2Related patent

US 9,067,966 B2Related patent

US 2011/0218204 A1This patent

From the US filing history. Foreign family members aren’t listed.

Pharmaceutically acceptable salts of novel betulinic acid derivatives

Life of this patent

Abstract

Claims26

Pharmaceutically acceptable salts of novel betulinic acid derivatives

Life of this patent

Abstract

Claims26