US4857513A
Expired / Lapsed
US
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Diphosphonic acid compounds, processes for the preparation thereof and pharmaceutical composition comprising the same
Assignee: Astellas Pharma Inc
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Filing: 1987-04-24
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Granted: 1989-08-15
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Expires: 2007-04-24
Abstract
Abstract A compound of the formula: <IMAGE> wherein R1-A- is a group of the formula: <IMAGE> in which R1 is aryl or a heterocyclic group, each of which may be substituted with substituent(s) selected from the group consisting of lower alkyl, lower alkoxy, lower alkylthio, halo(lower)alkyl, acyl, acylamino and halogen, or lower alkyl which may be substituted with a heterocyclic group optionally substituted with acyl, and X is O or S, and R2 is hydrogen or lower alkyl, provided that when R1 is lower alkyl, then R1-A- is a group of the formula: <IMAGE> in which R1 and X are each as defined above, and pharmaceutically acceptable salts thereof, processes for the preparation thereof and pharmaceutical composition comprising the same.
Inventors
- 👤 Teruo Oku
- 👤 Eishiro Todo
- 👤 Chiyoshi Kasahara
- 👤 Katsuya Nakamura
- 👤 Hiroshi Kayakiri
- 👤 Masashi Hashimoto
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-29 20:34
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; C07F9/60; C07F9/645; C07F9/6503; C07F9/6506; C07F9/6553; C07F9/655345; C07F9/655354
Claims Analysis
Total Claims: 9
Claim 1
Independent Claim
71 words
A compound of the formula: ##STR10## wherein R 1 --A-- is a group of the formula: ##STR11## in which R 1 is aryl or a heterocyclic group, each of which may be substituted with substituent(s) selected from the group consisting of lower alkyl, lower alkoxy, lower alkylthio, halo(lower)alkyl, acyl, acylamino and halogen, and X is O or S, and R 2 is hydrogen or lower alkyl, and pharmaceutically acceptable salts thereof.
Claim 2
Dependent Claim
71 words
A compound of the formula: ##STR10## wherein R 1 --A-- is a group of the formula: ##STR11## in which R 1 is aryl or a heterocyclic group, each of which may be substituted with substituent(s) selected from the group consisting of lower alkyl, lower alkoxy, lower alkylthio, halo(lower)alkyl, acyl, acylamino and halogen, and X is O or S, and R 2 is hydrogen or lower alkyl, and pharmaceutically acceptable salts thereof.
Claim 3
Dependent Claim
47 words
A compound of claim 1, wherein R 1 is phenyl, naphthyl, pyridyl, imidazolyl, thienyl, quinolyl, benzothienyl or benzothiazolyl, each of which may be substituted with substituent(s) selected from the group consisting of lower alkyl, lower alkoxy, lower alkylthio, halo(lower)alkyl, lower alkoxycarbonyl, lower alkanoylamino, lower alkylsulfonylamino and halogen.
Claim 4
Dependent Claim
62 words
A compound of claim 2, wherein R 1 --A-- is a group of the formula: ##STR12## in which R 1 is phenyl, naphthyl, lower alkylphenyl, lower alkoxyphenyl, lower alkylthiophenyl, mono or dihalophenyl, halo(lower)alkylphenyl, lower alkanoylaminophenyl, lower alkylsulfonylaminophenyl, halogen and halo(lower)alkyl substituted phenyl, lower alkoxy and halo(lower)alkyl substituted phenyl, pyridyl or, benzo[b]thienyl and X is O or S, and R 2 is hydrogen.
Claim 5
Dependent Claim
14 words
A compound of claim 3, wherein R 1 is phenyl, monohalophenyl, mono[halo(lower)alkyl]phenyl or mono(lower)alkylsulfonylaminophenyl.
Claim 6
Dependent Claim
12 words
A compound of claim 4, which is disodium salt of [N-(phenyl)thiocarbamoylmethylene]bis(phosphonic acid).
Claim 7
Dependent Claim
16 words
A compound of claim 2, wherein R 1 --A-- is a group of the formula: ##STR13##
Claim 8
Dependent Claim
30 words
A bone-resorption inhibitory pharmaceutical composition comprising, as an active ingredient, an effective amount of a compound of claim 1 or pharmaceutically acceptable salts thereof in association with a pharmaceutical carrier.
Claim 9
Dependent Claim
34 words
A method for the treatment of bone diseases characterized by abnormal bone metabolism in human beings or animals comprising administering an effective amount of a compound of claim 1 or pharmaceutically acceptable salts thereof.
References Cited (Backward Citations)
US3965254A
Cited
US4134969A
Cited
US3906062A
Cited
US4029697A
Cited
US4447256A
Cited
DE2741513A1
Cited
US4503049A
Cited
US4746654A
Cited
EP0100718A1
Cited
EP0170228A1
Cited
US4687767A
Cited
US4639338A
Cited
US4666895A
Cited
EP0210728A2
Cited
US4761406A
Cited
US4719203A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1992-08-14 | 1993-02-13 | 1993-08-15 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1996-08-14 | 1997-02-13 | 1997-08-15 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2000-08-14 | 2001-02-13 | 2001-08-15 | $7700.00 | Window Closed / Lapsed |