US4956381A
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Treating tissue calcium depletion or degenerative processes in bone or cartilage
Assignee: Sandoz AG
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Filing: 1988-10-25
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Granted: 1990-09-11
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Expires: 2008-10-25
Abstract
Abstract α-[10-oxy-4H-benzo[4,5]cycloheptal[1,2-b]thiophen-4-ylidene]-carboxylic acids, or physiologically-hydrolysable and -acceptable esters or pharmaceutically acceptable salts thereof are useful for effecting monokine inhibition, in particular interleukin-1 release or secretion inhibition, as a therapeutic means other than anti-inflammatory or anti-pyretic means.
Inventors
- 👤 Pietro Bollinger
- 👤 Hans U. Gubler
- 👤 Jorg Schnyder
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-08 22:33
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/33; A61K31/38; A61P; A61P3/00; A61P3/12; A61P3/14; A61P37/00; A61P37/02; A61P37/06; A61P43/00
Claims Analysis
Total Claims: 17
Claim 1
Independent Claim
102 words
A method of treating tissue calcium depletion or degenerative processes in bone or cartilage in a subject in need of said treatment, which comprises administering to said subject an effective amount for the treatment of tissue calcium depletion or degerative processes in bond or cartilage of a α-[b 10-oxy-4H-benzol[4,5]cyclohepta[1,2-b]thiophen-4-ylidene]-carboxylic acid of formula Ia ##STR3## wherein: R 1 is hydrogen or C 1-2 alkyl; and ring A is unsubstituted or halo- or hydroxy-substituted; or of formula Ib ##STR4## wherein: R 3 is C 1-2 alkyl and R 4 is halogen, or a physiologically hydrolysable and acceptable ester or a pharmaceutically acceptable salt thereof.
Claim 2
Independent Claim
102 words
A method of treating tissue calcium depletion or degenerative processes in bone or cartilage in a subject in need of said treatment, which comprises administering to said subject an effective amount for the treatment of tissue calcium depletion or degerative processes in bond or cartilage of a α-[b 10-oxy-4H-benzol[4,5]cyclohepta[1,2-b]thiophen-4-ylidene]-carboxylic acid of formula Ia ##STR3## wherein: R 1 is hydrogen or C 1-2 alkyl; and ring A is unsubstituted or halo- or hydroxy-substituted; or of formula Ib ##STR4## wherein: R 3 is C 1-2 alkyl and R 4 is halogen, or a physiologically hydrolysable and acceptable ester or a pharmaceutically acceptable salt thereof.
Claim 3
Dependent Claim
12 words
A method according to claim 1 for treating bone decalcification or resorption.
Claim 4
Dependent Claim
12 words
A method according claim 1 for treating odontal or periodontal calcium deficiency.
Claim 5
Dependent Claim
18 words
A method according to claim 1 for treating resorptive process or fibroblastic infiltration at or within bone joints.
Claim 6
Dependent Claim
8 words
A method to claim 1 for treating arthritis.
Claim 7
Dependent Claim
12 words
A method according to claim 1 for treating osteoarthritis or ankylosing spondylitis.
Claim 8
Dependent Claim
17 words
A method according to claim 1 for treating osteoporosis, osteopathy, osteomalacia or bone marrow healing and regeneration.
Claim 9
Dependent Claim
12 words
A method according to claim 1 for treating tetany or latent tetany.
Claim 10
Dependent Claim
39 words
A method of treating osteoarthritis which comprises administering an effective amount of a α-[10-oxy-4H-benzo [4,5]cyclohepta[1,2-b]thiophen-4ylidene]-carboxylic acid of formula Ia or Ib, as illustrated in claim 1, or a physiologically hydrolysable and acceptable ester or a pharmaceutically acceptable salt thereof.
Claim 11
Dependent Claim
40 words
A method of treating periodontal disease which comprises administering an effective amount of a α-[10-oxy-4H-benzo [4,5]cyclohepta[1,2-b]thiphen-4-ylidene]-carboxylic acid of formula Ia or Ib, as illustrated in claim 1, or a physiologically hydrolysable and acceptable ester or a pharmaceutically acceptable salt thereof.
Claim 12
Dependent Claim
38 words
A method according to claim 1, in which the 100 mg to 2.0 g of a compound of formula Ia or Ib or a physiologically hydrolysable and acceptable ester or a pharmaceutically acceptable salt thereof is administered daily.
Claim 13
Dependent Claim
39 words
A method according to claim 1, in which 25 mg to 1.0 g of a compound of formula ia or Ib or a physiologically hydrolysable and acceptable ester or a pharmaceutically acceptable salt thereof is administered per unit dose.
Claim 14
Dependent Claim
67 words
A method according to claim 1, wherein the α-[10-oxy-4H-benzo[4,5]cyclohepta[1,2-b]thiophen-4-ylidene]-carboxylic acid or physiologically-hydrolysable and -acceptable ester thereof is a compound selected from (A) [10-Methoxy-4H-benzo[4,5]cyclohepta[1,2-b]thiophen-4-ylidene]-acetic acid ethyl ester B) 7-Chloro-10-methoxy-4H-benzo4,5cyclohepta[1,2-b]-thiophen-4-ylidene]-acetic acid ethyl ester (C) [6-Hydroxy-10-methoxy-4H-benzo[4,5]cyclohepta[1,2-b]-thiophen-4-ylidene]-acetic acid ethyl ester (D) 10-Hethoxy-4H-benzo4,5cyclohepta[1,2-b]thiophen-4-ylidene-acetic acid (E) [10-Methoxy-4H-benzo4,5]cyclohepta[1,2-b]thiophen-4-ylidene-acetic acid methyl ester (F) [7-Chloro-10-methoxy-4H-benzo[4,5]cyclohepta[1,2-b]thiophen-4-ylidene]-acetic acid (G) [6-Hydroxy-10-methoxy-4H-benzo[4,5]cyclohepta[1,2-b]thiophen-4-ylidene]-acetic acid (H) [10-Hydroxy-4H-benzo[4,5]cyclohepta[1,2-b]thiophen-4-ylidene]-acetic acid (J) [2-Chloro-10-methoxy-4H-benzo[4,5]cyclohepta[1,2-b]thiophen-4-ylidene]-acetic acid ethyl ester (K) [2-Chloro-10-methoxy-4H-benzo[4,5]cyclohepta[1,2-b]thiophen-4-ylidene]-acetic acid or a pharmaceutically acceptable salt thereof.
Claim 15
Dependent Claim
19 words
A method according to claim 1, wherein the α-[10-oxy-4H-benzo[4,5]cyclohepta[1,2-b]thiophen-4-ylidene]-carboxylic acid is [10-methoxy-4H-benzo[4,5]cyclohepta[1,2-b]thiophen-4-ylidene]-acetic acid or a pharmaceutically acceptable salt thereof.
Claim 16
Dependent Claim
19 words
A method according to claim 1, wherein the α-[10-oxy-4H-benzo[4,5]cyclohepta[1,2-b]thiophen-4-ylidene]-carboxylic acid is [2-chloro-10-methoxy-4H-benzo[4,5]cyclohepta[1,2-b]thiophen-4-ylidene]-acetic acid or a pharmaceutically acceptable salt thereof.
Claim 17
Dependent Claim
28 words
A method according to claim 1, wherein the α-[10-oxy-4H-benzo[4,5]cyclohepta[1,2-b]thiophen-4-ylidene]-carboxylic acid or physiologically-hydrolysable and -acceptable ester or pharmaceutically acceptable salt thereof is in pure or substantially pure cis form.
References Cited (Backward Citations)
US4692460A
Cited
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