EP0186405B1
Expired / Lapsed
EP
⏱️ 0.0 years remaining
Pharmaceutical compositions containing geminal diphosphonates
Assignee: Procter and Gamble Co
•
Filing: 1985-12-16
•
Granted: 1991-03-06
•
Expires: 2005-12-16
Abstract
Abstract Pharmaceutical compositions, useful for treating abnormal calcium and phosphate metabolism, which contain geminal-diphosphonic acid compounds; and a method of treating diseases characterized by abnormal calcium and phosphate metabolism utilizing these pharmaceutical compositions.
Inventors
- 👤 James John Benedict
- 👤 Christopher Mark Perkins
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-10-31 15:44
CPC Classifications
C; C07; C07F; C07F9/00; C07F9/02; C07F9/28; C07F9/38; C07F9/3804; C07F9/3839; C07F9/3873; C07F9/547; C07F9/553; C07F9/576; C07F9/58; C07F9/645; C07F9/6509; C07F9/650905; C07F9/650952; C07F9/6512
Claims Analysis
Total Claims: 25
Claim 1
Independent Claim
268 words
A pharmaceutical composition for use in treatment of diseases characterised by abnormal calcium and phosphate metabolism, comprising: (a) from 0.001 mg P to 600 mg P of a geminal diphosphonic acid compound, or a pharmaceutically-acceptable salt or ester thereof, having the structure: wherein Z is a ring selected from the group consisting of pyridine, piridazine, pyrimidine and pyrazine; Q is oxygen, -NR 4 -, or a single bond; m + n is an integer from 0 to 5, provided that when Q is a single bond, m + n is 0 or 1; R 1 is hydrogen, substituted or unsubstituted amino, amido, hydroxy, alkoxy, halogen, carboxylate, substituted or unsubstituted, saturated or unsaturated hydrocarbon chain having from 1 to 6 carbon atoms, substituted or unsubstituted aryl, or substituted or unsubstituted benzyl, except that when n = 0 and Q is oxygen or NR 4 , then R 1 is hydrogen, substituted or unsubstituted, saturated or unsaturated hydrocarbon chain having from 1 to 6 carbon atoms, substituted or unsubstituted aryl, or substituted or unsubstituted benzyl; R 2 is hydrogen or substituted or unsubstituted, saturated or unsaturated hydrocarbon chain having from 1 to 4 carbon atoms; R 3 is one or more substituents selected from the group consisting of hydrogen, substituted and unsubstituted, saturated or unsaturated hydrocarbon chain having from 1 to 6 carbon atoms, substituted and unsubstituted aryl, substituted and unsubstituted benzyl, hydroxy, halogen, carbonyl, alkoxy, nitro, amido, amino, substituted amino, carboxylate, and combinations thereof, Ra. is hydrogen, substituted or unsubstituted, saturated or unsaturated hydrocarbon chain having from 1 to 4 carbon atoms, or acyl; and (b) a pharmaceutical carrier.
Claim 2
Dependent Claim
268 words
A pharmaceutical composition for use in treatment of diseases characterised by abnormal calcium and phosphate metabolism, comprising: (a) from 0.001 mg P to 600 mg P of a geminal diphosphonic acid compound, or a pharmaceutically-acceptable salt or ester thereof, having the structure: wherein Z is a ring selected from the group consisting of pyridine, piridazine, pyrimidine and pyrazine; Q is oxygen, -NR 4 -, or a single bond; m + n is an integer from 0 to 5, provided that when Q is a single bond, m + n is 0 or 1; R 1 is hydrogen, substituted or unsubstituted amino, amido, hydroxy, alkoxy, halogen, carboxylate, substituted or unsubstituted, saturated or unsaturated hydrocarbon chain having from 1 to 6 carbon atoms, substituted or unsubstituted aryl, or substituted or unsubstituted benzyl, except that when n = 0 and Q is oxygen or NR 4 , then R 1 is hydrogen, substituted or unsubstituted, saturated or unsaturated hydrocarbon chain having from 1 to 6 carbon atoms, substituted or unsubstituted aryl, or substituted or unsubstituted benzyl; R 2 is hydrogen or substituted or unsubstituted, saturated or unsaturated hydrocarbon chain having from 1 to 4 carbon atoms; R 3 is one or more substituents selected from the group consisting of hydrogen, substituted and unsubstituted, saturated or unsaturated hydrocarbon chain having from 1 to 6 carbon atoms, substituted and unsubstituted aryl, substituted and unsubstituted benzyl, hydroxy, halogen, carbonyl, alkoxy, nitro, amido, amino, substituted amino, carboxylate, and combinations thereof, Ra. is hydrogen, substituted or unsubstituted, saturated or unsaturated hydrocarbon chain having from 1 to 4 carbon atoms, or acyl; and (b) a pharmaceutical carrier.
Claim 3
Dependent Claim
37 words
A pharmaceutical composition according to claim 1 wherein the geminal diphosphonic acid compound has the structure: wherein R 1 to R 3 , m + n, and Z m + n are as defined in claim 1.
Claim 4
Dependent Claim
33 words
A pharmaceutical composition according to claim 1 wherein the geminal diphosphonic acid compound has the structure: wherein R 1 to R 4 , m, n and Z are as defined in claim 1.
Claim 5
Dependent Claim
32 words
A pharmaceutical composition according to claim 1 wherein the geminal diphosphonic acid compound has the structure: wherein R 1 to R 3 , m,n, and Z are as defined in claim 1.
Claim 6
Dependent Claim
16 words
A pharmaceutical composition according to Claim 2, 3 or 4, wherein Z is pyridine or pyrimidine.
Claim 7
Dependent Claim
16 words
A pharmaceutical composition according to Claim 2, 3 or 4, wherein m + n = 1.
Claim 8
Dependent Claim
13 words
A pharmaceutical composition according to Claim 2, wherein m + n = 2.
Claim 9
Dependent Claim
15 words
A pharmaceutical composition according to Claim 3 or 4, wherein m + n = 0.
Claim 10
Dependent Claim
17 words
A pharmaceutical composition according to Claim 2, wherein Z is pyridine and m + n = 1.
Claim 11
Dependent Claim
19 words
A pharmaceutical composition according to Claim 3, wherein Z is pyridine or pyrimidine, and m + n = 0
Claim 12
Dependent Claim
79 words
A pharmaceutical composition according to Claim 2 comprising : (a) from 0.001 mg P to 600 mg P of a geminal diphosphonic acid compound, or a pharmaceutically-acceptable salt or ester thereof, having the structure : wherein m + n = 0 or 1; R 1 is hydrogen, chloro, amino, or hydroxy; R 3 is one or more substituents selected from the group consisting of hydrogen, methyl, amino, chloro, methoxy, hydroxy, nitro, and combinations thereof; and (b) a pharmaceutical carrier.
Claim 13
Dependent Claim
77 words
A pharmaceutical composition according to Claim 2 comprising : (a) from 0.001 mg P to 600 mg P of a geminal diphosphonic acid compound, or a pharmaceutically-acceptable salt or ester thereof, having the structure : wherein m+n = 0 or 1; R 1 is hydrogen, chloro, amino, or hydroxy; R 3 is one or more substituents selected from the group consisting of hydrogen, methyl, amino, chloro, methoxy, hydroxy, nitro, and combinations thereof; and (b) a pharmaceutical carrier.
Claim 14
Dependent Claim
97 words
A pharmaceutical composition according to Claim 3 comprising : (a) from 0.001 mg P to 600 mg P of a geminal diphosphonic acid compound, or a pharmaceutcially- acceptable salt or ester thereof, having the structure : wherein n + 0 or 1; R 1 is hydrogen, chloro, amino, or hydroxy when n = I, and R 1 is hydrogen when n=0; R 3 is one or more substituents selected from the group consisting of hydrogen, methyl, amino, chloro, methoxy, nitro, hydroxy, and combinations thereof; and R 4 is hydrogen, methyl, or ethyl; and (b) a pharmaceutical carrier.
Claim 15
Dependent Claim
96 words
A pharmaceutical composition according to Claim 3 comprising : (a) from 0.001 mg P to 600 mg P of a geminal diphosphonic acid compound, or a pharmaceutically-acceptable salt or ester thereof, having the structure : wherein n = 0 or 1; R 1 is hydrogen, chloro, amino, or hydroxy when n = 1, and R 3 is hydrogen when n=0; R 3 is one or more substituents selected from the group consisting of hydrogen, methyl, amino, chloro, methoxy, nitro, hydroxy, and combinations thereof; and R 4 is hydrogen, methyl, or ethyl; and (b) a pharmaceutical carrier.
Claim 16
Dependent Claim
88 words
A pharmaceutical composition according to Claim 4 comprising : (a) from 0.001 mg P to 600 mg P of a geminal diphosphonic acid compound, or a pharmaceutically-acceptable salt or ester thereof, having the structure : wherein n = 0 or 1; R 1 is hydrogen, chloro, amino, or hydroxy when n = 1, and R 1 is hydrogen when n=0; R 3 is one or more substituents selected from the group consisting of hydrogen, methyl, amino, chloro, methoxy, nitro, hydroxy, and combinations thereof; and (b) a pharmaceutical carrier.
Claim 17
Dependent Claim
88 words
A pharmaceutical composition according to Claim 4 comprising : (a) from 0.001 mg P to 600 mg P of a geminal diphosphonic acid compound, or a pharmaceutically-acceptable salt or ester thereof, having the structure : herein n = 0 or 1; R 1 is hydrogen, chloro, amino, or hydroxy when n = 1, and R 1 is hydrogen when n=0; R 3 is one or more substituents selected from the group consisting of hydrogen, methyl, amino, chloro, methoxy, nitro, hydroxy, and combinations thereof; and (b) a pharmaceutical carrier.
Claim 18
Dependent Claim
75 words
A pharmaceutical compositon according to claim 1 comprising: (a) from 0.001 mg P to 600 mg P of a geminal diphosphonic acid compound, or a pharmaceutically-acceptable salt or ester thereof, selected from the group consisting of N-(2-(5-amino)-pyridyl)-aminomethane diphosphonic acid; N-(2-(5-chloro)-pyridyl)-aminomethane diphosphonic acid; N-(2-(3-picolyl))-aminomethane diphosphonic acid; N-(2-(4-picolyl))-aminomethane diphosphonic acid; N-(2-(5-picolyl))-aminomethane diphosphonic acid; N-(2-(6-picolyl))-aminomethane diphosphonic acid; N-(2-(3,4-lutidine))-aminomethane diphosphonic acid; N-(2-pyrimidyl)-aminomethane diphosphonic acid; N-(2-pyridyl)-2-aminomethane-I,I-diphosphonic acid; 2-(2-pyridyl)-ethane-1,1-diphosphonic acid; 2-(3-pyridyl)-ethane-1,1-diphosphonic acid; 2-(4-pyridyl)-ethane-1,1-diphosphonic acid; 0-(2-(3-picolyl))-2-oxa-ethane-1,1-diphosphonic acid; and (b) a pharmaceutical carrier.
Claim 19
Dependent Claim
34 words
A pharmaceutical composition according to Claim 1 comprising : (a) from 0.001 mg P to 600 mg P of N-(2-(3-picolyl))-aminomethane diphosphonic acid, or a pharmaceutically-acceptable salt or ester thereof; and (b) a pharmaceutical carrier.
Claim 20
Dependent Claim
33 words
A pharmaceutical composition according to Claim 1, comprising : (a) from 0.001 mg P to 600 mg P of 2-(2-pyridyl)-ethane-1,1-diphosphonic acid, or a pharmaceutically-acceptable salt or ester thereof; and (b) a pharmaceutical carrier.
Claim 21
Dependent Claim
156 words
Diphosphonic acid compounds having the structure : wherein Z is a ring selected from the group consisting of pyridine, pyridazine, pyrimidine and pyrazine; R 1 is hydrogen, substituted or unsubstituted amino, amido, hydroxy, alkoxy, halogen, carboxylate, substituted or unsubstituted, saturated or unsaturated hydrocarbon chain having from 1 to 6 carbon atoms, substituted or unsubstituted aryl, or substituted or unsubstituted benzyl; R 2 is hydrogen, or substituted or unsubstituted, saturated or unsaturated hydrocarbon chain having from 1 to 4 carbon atoms; R 3 is one or more substituents selected from the group consisting of hydrogen, substituted and unsubstituted, saturated or unsaturated hydrocarbon chain having from 1 to 6 carbon atoms, substituted and unsubstituted aryl, substituted and unsubstituted benzyl, hydroxy, halogen, carbonyl, alkoxy, nitro, amido, amino, substituted amino, carboxylate, and combinations thereof; Ra. is hydrogen, substituted or unsubstituted, saturated or unsaturated hydrocarbon chain having from 1 to 4 carbon atoms, or acyl; and pharmaceutically-acceptable salts and esters thereof.
Claim 22
Dependent Claim
156 words
Diphosphonic acid compounds having the structure : wherein Z is a ring selected from the group consisting of pyridine, pyridazine, pyrimidine and pyrazine; R 1 is hydrogen, substituted or unsubstituted amino, amido, hydroxy, alkoxy, halogen, carboxylate, substituted or unsubstituted, saturated or unsaturated hydrocarbon chain having from 1 to 6 carbon atoms, substituted or unsubstituted aryl, or substituted or unsubstituted benzyl; R 2 is hydrogen, or substituted or unsubstituted, saturated or unsaturated hydrocarbon chain having from 1 to 4 carbon atoms; R 3 is one or more substituents selected from the group consisting of hydrogen, substituted and unsubstituted, saturated or unsaturated hydrocarbon chain having from 1 to 6 carbon atoms, substituted and unsubstituted aryl, substituted and unsubstituted benzyl, hydroxy, halogen, carbonyl, alkoxy, nitro, amido, amino, substituted amino, carboxylate, and combinations thereof; Ra. is hydrogen, substituted or unsubstituted, saturated or unsaturated hydrocarbon chain having from 1 to 4 carbon atoms, or acyl; and pharmaceutically-acceptable salts and esters thereof.
Claim 23
Dependent Claim
102 words
Diphosphonic acid compounds having the structure : wherein Z is a ring selected from the group consisting of pyridine, pyridazine, pyrimidine and pyrazine; n is 1; R 2 is hydrogen, or substituted or unsubstituted, saturated or unsaturated hydrocarbon chain having from 1 to 4 carbon atoms; and R 3 is one or more substituents selected from the group consisting of hydrogen, substituted and unsubstituted,saturated or unsaturated hydrocarbon chain having from 1 to 6 carbon atoms, substituted and unsubstituted aryl, substituted and unsubstituted benzyl, hydroxy, halogen, carbonyl, alkoxy, nitro, amido, amino, substituted amino, carboxylate, and combinations thereof; and pharmaceutically-acceptable salts and esters thereof.
Claim 24
Dependent Claim
102 words
Diphosphonic acid compounds having the structure : wherein Z is a ring selected from the group consisting of pyridine, pyridazine, pyrimidine and pyrazine; n is 1; R 2 is hydrogen, or substituted or unsubstituted, saturated or unsaturated hydrocarbon chain having from 1 to 4 carbon atoms; and R 3 is one or more substituents selected from the group consisting of hydrogen, substituted and unsubstituted,saturated or unsaturated hydrocarbon chain having from 1 to 6 carbon atoms, substituted and unsubstituted aryl, substituted and unsubstituted benzyl, hydroxy, halogen, carbonyl, alkoxy, nitro, amido, amino, substituted amino, carboxylate, and combinations thereof; and pharmaceutically-acceptable salts and esters thereof.
Claim 25
Dependent Claim
11 words
Diphosphonic acid compounds according to Claim 21 wherein Z is pyridine.
References Cited (Backward Citations)
No citation records indexed.
USPTO Annuity & Maintenance Windows
Maintenance schedule is calculated for granted US utility patents.