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EP0619116A2 Expired / Lapsed EP ⏱️ 0.0 years remaining

Use of synthetic retinoids for osteopathy

Assignee: Shudo Koichi Prof Dr
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Filing: 1994-03-30
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Granted: —
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Expires: 2014-03-30
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Abstract

Abstract An anti-osteopathic composition comprising as an active ingredient a compound represented by the following formula (I), (II) or (III): which is useful for therapeutic and prophylactic treatment of osteopathia such as osteoporosis and bone fracture.

Inventors

  • 👤 Koichi Shudo
  • 👤 Tatsuo Sugioka
  • 👤 Mizuho Inazu
  • 👤 Hideyuki Tanaka
  • 👤 Tsutomu Inoue
  • 👤 Kazuyuki Kitamura

Bibliographic Details

Application Number —
Jurisdiction EP
Data Source google_patents
Last Synchronized 2026-11-02 15:27
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/655; A61K31/185; A61K31/19; A61K31/192; A61K31/195; A61K31/196; A61K31/33; A61K31/335; A61K31/336; A61K31/35; A61K31/352; A61K31/395; A61K31/435; A61K31/44

Claims Analysis

Total Claims: 10
Claim 1
Independent Claim 191 words
An anti-osteopathic composition comprising as an active ingredient a compound of the formula (I): wherein R₁, R₂, R₃, R₄ and R₅ independently represent a hydrogen atom, a lower or middle alkyl group, or a lower or middle alkoxy group, with the proviso that all of R₁, R₂, R₃, R₄ and R₅ do not simultaneously represent hydrogen atoms, any two adjacent groups selected from these groups may combine to form a 5- or 6-membered cycloalkyl ring together with carbon atoms substituted by those groups and the cycloalkyl ring may further be substituted with one or more lower alkyl groups; R₆ represents a hydroxyl group, a lower alkoxy group, or -NR₇R₈ group in which R₇ and R₈ independently represent a hydrogen atom or a lower alkyl group; X represents a radical selected from the group consisting of the radicals represented by the following formulas: and wherein R₉ and R₁₀ independently represents a hydrogen atom or a lower alkyl group and; Y represents a radical selected from the group consisting of the radicals represented by the following formulas: wherein W represents a hydrogen atom or a hydroxy group, or a salt of said compound.
Claim 2
Dependent Claim 120 words
The anti-osteopathic composition according to claim 1, wherein the active ingredient is a compound or a salt of the compound selected from the group consisting of 4-[(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl) carboxamide]benzoic acid (hereinafter referred to as "Am580"), 4-[(3,4-diisopropylphenyl)carboxamide]benzoic acid, 5-[(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)carboxamide]pyridine-2-carboxylic acid, 6-[(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)carboxamide]pyridine-3-carboxylic acid, 3-hydroxy-4-[(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)carboxamide]benzoic acid (hereinafter referred to as "Am589"), 4-[(3-isopropyl-4-isopropoxyphenyl)carboxamide]benzoic acid (hereinafter referred to as "Am685"), 3-hydroxy-4-[(3-isopropyl-4-isopropoxyphenyl)carboxamide]-benzoic acid (hereinafter referred to as "Am689"), 4-[(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)carbamoyl]benzoic acid (hereinafter referred to as "Am80"), 4-[(3,4-diisopropylphenyl)carbamoyl]benzoic acid, 5-[(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)carbamoyl]pyridine-2-carboxylic acid, (E)-4-[3-(3,5-di-tert-butylphenyl)-3-oxo-1-propenyl]benzoic acid (hereinafter referred to as "Ch55"), (E)-4-[3-(3,5-diisopropylphenyl)-3-oxo-1-propenyl]benzoic acid, 6-[(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)carbamoyl]pyridine-3-carboxylic acid (hereinafter referred to as "R300"), 4-[3-methyl-3-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)oxylanyl]benzoic acid, 4-[(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)azoxy]benzoic acid, 4-[(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)azo]benzoic acid, 4-[(3,5-di-tert-butylphenyl)carboxamide]benzoic acid, 4-[(3,5-di-tert-butylphenyl)carbamoyl]benzoic acid, 5-[(3,4-diisopropylphenyl)carboxamide]pyridine-2-carboxylic acid, 6-[(3,4-diisopropylphenyl)carboxamide]pyridine-3-carboxylic acid, 5-[(3,4-diisopropylphenyl)carbamoyl]pyridine-2-carboxylic acid, 6-[(3,4-diisopropylphenyl)carbamoyl]pyridine-3-carboxylic acid, 4-[3-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)-oxyranyl]benzoic acid (hereinafter referred to as "Ep80"), 4-[(3,4-diisopropylphenyl)azo]benzoic acid (hereinafter referred to as "Az68").
Claim 3
Dependent Claim 17 words
The anti-osteopathic composition according to claim 1 or 2, wherein the active ingredient is 4-[(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)carboxamide]benzoic acid (Am580).
Claim 4
Dependent Claim 97 words
An anti-osteopathic composition comprising as an active ingredient a compound of formula (II) or (III) wherein R₁₁ and R₁₂ independently represent a hydrogen atom or a lower or middle alkyl group or R₁₁ and R₁₂ may combine to form a 6-membered cycloalkyl ring together with carbon atoms substituted by these groups and said cycloalkyl ring may contain an oxygen atom and may be substituted by one or more lower alkyl groups; R₁₃ represents a hydrogen atom or a lower alkyl group; and W represents a hydrogen atom or a hydroxy group, or a salt of said compound.
Claim 5
Dependent Claim 46 words
The anti-osteopathic composition as claimed in claim 4, wherein the active ingredient is a compound or a salt thereof selected from the group consisting of 4-(6,7,8,9-tetrahydro-3-hydroxy-6,6,9,9-tetramethyl-4H-4-oxonaphtho[2.3-b]pyran-2-yl)benzoic acid (hereinafter referred to as "Fv180"), 4-(6,7,8,9-tetrahydro-6,6,9,9-tetramethyl-4H-4-oxonaphtho[2.3-b]pyran-2-yl)-benzoic acid (hereinafter referred to as "Fv80"), 4-[1-hydroxy-3-oxo-3-(5,6,7,8-tetrahydro-3-hydroxy-5,5,8,8-tetramethyl-2-naphthalenyl)-1-propenyl]benzoic acid (hereinafter referred to as "Re80").
Claim 6
Dependent Claim 15 words
The anti-osteopathic composition according to claims 1 - 5 useful for therapeutic treatment of osteopathia.
Claim 7
Dependent Claim 16 words
The anti-osteopathic composition according to claim 6 wherein the osteopathia is osteoporosis or a bone fracture.
Claim 8
Dependent Claim 15 words
The anti-osteopathic composition according to claims 1 - 5 useful for prophylactic treatment of osteopathia.
Claim 9
Dependent Claim 12 words
The anti-osteopathic composition according to claim 8 wherein the osteopathia is osteoporosis.
Claim 10
Dependent Claim 23 words
A compound selected from the group consisting of 4-[(3-isopropyl-4-isopropoxyphenyl)carboxamide]benzoic acid (hereinafter referred to as "Am685") and 3-hydroxy-4-[(3-isopropyl-4-isopropoxyphenyl)carboxamide]-benzoic acid (hereinafter referred to as "Am689").

References Cited (Backward Citations)

EP0170105A2 Cited
EP0232199A2 Cited

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