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EP0148752A2 Expired / Lapsed EP ⏱️ 0.0 years remaining

Protease inhibitors

Assignee: GD Searle LLC
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Filing: 1985-01-08
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Granted: —
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Expires: 2005-01-08
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Abstract

Abstract This invention relates to compositions for preventing or reducing the degradation of elastin and other proteins and thereby preventing or retarding the disease states caused by said degradation containing as active ingredients compounds, some of which are novel, of the formula: or their pharmacologically acceptable salts.

Inventors

  • 👤 Richard August Mueller
  • 👤 Richard Allen Partis

Bibliographic Details

Application Number —
Jurisdiction EP
Data Source google_patents
Last Synchronized 2026-10-25 11:41
CPC Classifications
C; C07; C07C; C07C69/00; C07C69/52; C07C69/533; A; A61; A61P; A61P43/00; C07C57/00; C07C57/02; C07C57/03; C07C57/12

Claims Analysis

Total Claims: 19
Claim 1
Independent Claim 213 words
A composition for preventing or reducing the degradation of elastin and other proteins and thereby preventing or retarding the disease states caused by said degradation containing as active ingredients compounds of the formula: wherein R is: a) alkyl of 15 to 19 carbon atoms, inclusive; being saturated, unsaturated or polyunsaturated; wherein R 2 is: a) hydrogen; b) alkyl of 1 to 6 carbon atoms, inclusive; or c) phenyl or phenyl methyl wherein the phenyl portion may optionally be substituted by Y and Z; wherein Y and Z each being the same or different are: a) hydrogen; b) halogen; c) alkyl of 1 to 6 carbon atoms, inclusive; d) hydroxy; e) methoxy; f) acetoxy; g) carboxylic acid and its alkyl esters of 1 to 6 carbon atoms, inclusive; h) nitro; or i) phenyl; wherein M is: a) phenyl substituted by X and W; b) methylene; wherein W and X each being the same or different are: a) hydrogen; b) alkyl of from 1 to 6 carbon atoms, inclusive; c) hydroxy; d) methoxy; e) carboxylic acid and its alkyl esters of from 1 to 6 carbon atoms inclusive; f) halogen; g ) -N0 2 ; or h) acetoxy; wherein when W and X are contiguous they may be taken together to form a phenyl ring.
Claim 2
Dependent Claim 213 words
A composition for preventing or reducing the degradation of elastin and other proteins and thereby preventing or retarding the disease states caused by said degradation containing as active ingredients compounds of the formula: wherein R is: a) alkyl of 15 to 19 carbon atoms, inclusive; being saturated, unsaturated or polyunsaturated; wherein R 2 is: a) hydrogen; b) alkyl of 1 to 6 carbon atoms, inclusive; or c) phenyl or phenyl methyl wherein the phenyl portion may optionally be substituted by Y and Z; wherein Y and Z each being the same or different are: a) hydrogen; b) halogen; c) alkyl of 1 to 6 carbon atoms, inclusive; d) hydroxy; e) methoxy; f) acetoxy; g) carboxylic acid and its alkyl esters of 1 to 6 carbon atoms, inclusive; h) nitro; or i) phenyl; wherein M is: a) phenyl substituted by X and W; b) methylene; wherein W and X each being the same or different are: a) hydrogen; b) alkyl of from 1 to 6 carbon atoms, inclusive; c) hydroxy; d) methoxy; e) carboxylic acid and its alkyl esters of from 1 to 6 carbon atoms inclusive; f) halogen; g ) -N0 2 ; or h) acetoxy; wherein when W and X are contiguous they may be taken together to form a phenyl ring.
Claim 3
Dependent Claim 191 words
Compounds of the formula: wherein R is: a) alkyl of 15 to 19 carbon atoms, inclusive; being saturated, unsaturated or polyunsaturated; wherein R 2 is: a) alkyl of 1 to 6 carbon atoms, inclusive; or b) phenyl or phenyl methyl wherein the phenyl portion may optionally be substituted by Y and Z; wherein Y and Z each being the same or different are: a) hydrogen; b) halogen; c) alkyl of 1 to 6 carbon atoms, inclusive; d) hydroxy; e) methoxy; f) acetoxy; g) carboxylic acid and its alkyl esters of 1 to 6 carbon atoms, inclusive; h) nitro; or i) phenyl; wherein M is: a) phenyl substituted by X and W; b) methylene; wherein W and X each being the same or different are: a) hydrogen; b) alkyl of from 1 to 6 carbon atoms, inclusive; c) hydroxy; d) methoxy.; e) carboxylic acid and its alkyl esters of from 1 to 6 carbon atoms inclusive; f) halogen; g) -NO 2 ; or h) acetoxy; wherein when W and X are contiguous they may be taken together to form a phenyl ring; and wherein W and X may not both be hydrogen.
Claim 4
Dependent Claim 191 words
Compounds of the formula: wherein R is: a) alkyl of 15 to 19 carbon atoms, inclusive; being saturated, unsaturated or polyunsaturated; wherein R 2 is: a) alkyl of 1 to 6 carbon atoms, inclusive; or b) phenyl or phenyl methyl wherein the phenyl portion may optionally be substituted by Y and Z; wherein Y and Z each being the same or different are: a) hydrogen; b) halogen; c) alkyl of 1 to 6 carbon atoms, inclusive; d) hydroxy; e) methoxy; f) acetoxy; g) carboxylic acid and its alkyl esters of 1 to 6 carbon atoms, inclusive; h) nitro; or i) phenyl; wherein M is: a) phenyl substituted by X and W; b) methylene; wherein W and X each being the same or different are: a) hydrogen; b) alkyl of from 1 to 6 carbon atoms, inclusive; c) hydroxy; d) methoxy.; e) carboxylic acid and its alkyl esters of from 1 to 6 carbon atoms inclusive; f) halogen; g) -NO 2 ; or h) acetoxy; wherein when W and X are contiguous they may be taken together to form a phenyl ring; and wherein W and X may not both be hydrogen.
Claim 5
Dependent Claim 17 words
Compounds according to Claim 2 wherein R 2 is alkyl of 1 to 6 carbon atoms, inclusive.
Claim 6
Dependent Claim 8 words
2-[methyl(1-oxo-9Z-octadecenyl)amino]benzoic acid a compound according to Claim 3.
Claim 7
Dependent Claim 8 words
2-hydroxy-5-[methyl(1-oxo-9Z-octadecenyl)amino]benzoic acid a compound according to Claim 3.
Claim 8
Dependent Claim 11 words
A compound according to Claim 2 wherein R 2 is phenyl.
Claim 9
Dependent Claim 7 words
N-(4-chlorophenyl)-N-(1-oxo-9Z-octadecenyl)glycine a compound according to Claim 6.
Claim 10
Dependent Claim 7 words
N-(4-hydroxyphenyl)-N-(1-oxo-9Z-octadecenyl)glycine a compound according to Claim 6.
Claim 11
Dependent Claim 7 words
N-(l-oxo-9Z-octadecenyl)-N-phenylglycine a compound according to Claim 6.
Claim 12
Dependent Claim 7 words
N-(2-hydroxyphenyl)-N-(1-oxo-9Z-octadecenyl)glycine a compound according to Claim 6.
Claim 13
Dependent Claim 12 words
A compound according to Claim 2 wherein R 2 is phenyl alkyl.
Claim 14
Dependent Claim 7 words
N-(1-oxo-9Z-octadecenyl)-N-(phenylmethyl)glycine a compound according to Claim 11.
Claim 15
Dependent Claim 8 words
N-[(3,4-dichlorophenvl)methyl]-N-(1-oxo-9Z-octadecenyl) glycine a compound according to Claim 11.
Claim 16
Dependent Claim 8 words
N-[(2-chlorophenyl)methyl)-N-(1-oxo-9Z-octadecenyl) glycine a compound according to Claim 11.
Claim 17
Dependent Claim 8 words
N-([1,1'-biphenyl)-4-ylmethyl)-N-(1-oxo-9Z-octadecenyl) glycine a compound according to Claim 11.
Claim 18
Dependent Claim 8 words
N-[(4-iodophenyl)methyl]-N-(1-oxo-9Z-octadecenyl) glycine a compound according to Claim 11.
Claim 19
Dependent Claim 8 words
N-[(4-chlorophenyl)methyl]-N-(1-oxo-9Z-octadecenyl) glycine a compound according to Claim 11.

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