Patent · US5122520A · A · US
Acid addition salts of amidated taurine or glycine, their preparation and use
- (11) Publication number
- US5122520A
- (21) Application number
- US-65978891-A
- (22) Filing date
- 1991-02-22
- (30) Priority date
- 1988-04-30
- (43) Publication date
- 1992-06-16
- (45) Date of grant
- 1992-06-16
- (52) CPC
- (73) Assignee
- SANDOZ LTD
- (54) Title
- Acid addition salts of amidated taurine or glycine, their preparation and use
- (57) Abstract
Acid addition salt of taurine or glycine, their amino group being amidated with a carboxylic acid residue which contains the structure of a 3 alpha, 7 alpha, 12 alpha -trihydroxysteroid, their acid group being neutralized with the amino group of an aliphatic amine or neutralized with the amino group of a basic alpha -amino carboxylic acid which group is connected over an alkylene bridge with the alpha -amino acid group, may be used e.g. as transmucuous resorption promoter of drug compounds.
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Claims (15)
- An acid addition salt of an anion (i) of taurine or glycine wherein the amino group thereof is substituted by an acyl group of a 3α,7α,12α-trihydroxy steroid carboxylic acid and a cation (ii) of either (a) an aliphatic amine any substituents of which are other than carboxyl groups or (b) a basic alpha amino acid having an alkylene bridge between the alpha amino acid group and another amino group.
- A salt of claim 1 wherein the anion is derived from taurocholic or glycocholic acid.
- A salt of claim 1 wherein the cation is derived from a basic alpha amino acid having an alkylene bridge between the alpha amino acid group and another amino group.
- A salt of claim 3 wherein the cation is derived from lysine.
- An acid addition salt of an anion of formula II ##STR7## in which R 1 =H or OH and R 2 =--CH 2 --COO - or --CH 2 --CH 2 --SO 3 - and a cation having the formula ##STR8##
- A salt of claim 5 wherein R 1 is hydrogen.
- A salt of claim 6 wherein R 2 is --CH 2 --CH 2 --SO 3 -.
- A pharmaceutical composition comprising at least one pharmacologically active agent and an acid addition salt of claim 1.
- A composition according to claim 8 wherein the pharmacologically active agent is a calcitonin.
- A composition according to claim 8 wherein the ratio of acid addition salt to pharmacologically active agent is from 1:1 to 5000:1.
- A composition according to claim 8 in unit dosage form containing from about 0.1 to 100 mg of the acid addition salt.
- A composition according to claim 8 in nasal form.
- A composition according to claim 8 comprising an acid addition salt of an anion of formula II ##STR9## wherein R 1 is hydrogen or hydroxy, and R 2 is --CH 2 --COO - or --CH 2 --CH 2 --SO 3 -, and a cation having the formula ##STR10##
- A composition according to claim 13 wherein R 1 is hydrogen.
- A composition according to claim 14 wherein R 2 is --CH 2 --CH 2 --SO 3 -.
Citations (5)
- US3580936A
- US3839565A
- US3856953A
- US4104285A
- US4746508A
Record as JSON
{
"publication_number": "US5122520A",
"country": "US",
"kind": "A",
"title": "Acid addition salts of amidated taurine or glycine, their preparation and use",
"abstract": "Acid addition salt of taurine or glycine, their amino group being amidated with a carboxylic acid residue which contains the structure of a 3 alpha, 7 alpha, 12 alpha -trihydroxysteroid, their acid group being neutralized with the amino group of an aliphatic amine or neutralized with the amino group of a basic alpha -amino carboxylic acid which group is connected over an alkylene bridge with the alpha -amino acid group, may be used e.g. as transmucuous resorption promoter of drug compounds.",
"claims": [
"1. An acid addition salt of an anion (i) of taurine or glycine wherein the amino group thereof is substituted by an acyl group of a 3α,7α,12α-trihydroxy steroid carboxylic acid and a cation (ii) of either (a) an aliphatic amine any substituents of which are other than carboxyl groups or (b) a basic alpha amino acid having an alkylene bridge between the alpha amino acid group and another amino group.",
"2. A salt of claim 1 wherein the anion is derived from taurocholic or glycocholic acid.",
"3. A salt of claim 1 wherein the cation is derived from a basic alpha amino acid having an alkylene bridge between the alpha amino acid group and another amino group.",
"4. A salt of claim 3 wherein the cation is derived from lysine.",
"5. An acid addition salt of an anion of formula II ##STR7## in which R 1 =H or OH and R 2 =--CH 2 --COO - or --CH 2 --CH 2 --SO 3 - and a cation having the formula ##STR8##",
"6. A salt of claim 5 wherein R 1 is hydrogen.",
"7. A salt of claim 6 wherein R 2 is --CH 2 --CH 2 --SO 3 -.",
"8. A pharmaceutical composition comprising at least one pharmacologically active agent and an acid addition salt of claim 1.",
"9. A composition according to claim 8 wherein the pharmacologically active agent is a calcitonin.",
"10. A composition according to claim 8 wherein the ratio of acid addition salt to pharmacologically active agent is from 1:1 to 5000:1.",
"11. A composition according to claim 8 in unit dosage form containing from about 0.1 to 100 mg of the acid addition salt.",
"12. A composition according to claim 8 in nasal form.",
"13. A composition according to claim 8 comprising an acid addition salt of an anion of formula II ##STR9## wherein R 1 is hydrogen or hydroxy, and R 2 is --CH 2 --COO - or --CH 2 --CH 2 --SO 3 -, and a cation having the formula ##STR10##",
"14. A composition according to claim 13 wherein R 1 is hydrogen.",
"15. A composition according to claim 14 wherein R 2 is --CH 2 --CH 2 --SO 3 -."
],
"cpc": [
"A61K 47/28",
"C07J 41/0061"
],
"assignees": [
"SANDOZ LTD"
],
"filing_date": "1991-02-22",
"publication_date": "1992-06-16",
"grant_date": "1992-06-16",
"priority_date": "1988-04-30",
"application_number": "US-65978891-A",
"family_id": "6353289",
"citations": [
"US3580936A",
"US3839565A",
"US3856953A",
"US4104285A",
"US4746508A"
]
}
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