Compounds and methods for the treatment of pain and other diseases
AssigneeAquilus Pharmaceuticals, Inc.
InventorIrving Sucholeiki
Life of this patent
Estimating the term…
Abstract
The present invention relates generally to alkyne containing pharmaceutical agents, and in particular, to phenylethynyl-thiophene based metalloprotease inhibitor compounds. More particularly, the present invention provides a new class of MMP inhibiting compounds that exhibit increased potency, metabolic stability and/or reduced toxicity in relation to currently known MMP inhibitors for the treatment of pain and other diseases such as cancer. Additionally, the present invention relates to methods for treating pain in a patient comprising administering to the patient a pain-reducing effective amount of a present compound.
Claims21
1-3. (canceled)
A compound having Formula (II):
- wherein:
- each of R1, R2, R3, R4, R5, R6, R7, R8 R9, R10, R11, R12, R13, R14, R15 R16, and R17 is independently selected from the group consisting of deuterium, hydrogen, alkyl, hydroxyl and deuteroalkyl;
- and
- R18 is independently selected from the group consisting of hydrogen, deuterium, alkyl, deuteroalkyl, sodium, potassium;
- or
- N-oxides, pharmaceutically acceptable salts, prodrugs, formulations, polymorphs, tautomers, racemic mixtures or stereoisomers thereof.
The compound of claim 1, wherein said compound is selected from the group consisting of:
- or a pharmaceutically acceptable salt thereof.
6-22. (canceled)
A method of inhibiting a metalloproteinase enzyme, comprising administering to a subject in need thereof a compound of Formula (II):
- wherein:
- each of R1, R2, R3, R4, R5, R6, R7, R8 R9, R10, R11, R12, R13, R14, R15 R16, and R17 is independently selected from the group consisting of deuterium, hydrogen, alkyl, and deuteroalkyl;
- R18 is independently selected from the group consisting of hydrogen, deuterium, alkyl, deuteroalkyl, sodium, and potassium;
- or
- N-oxides, pharmaceutically acceptable salts, prodrugs, formulations, polymorphs, tautomers, racemic mixtures or stereoisomers thereof.
(canceled)
A method of treating an MMP mediated condition, comprising administering to a subject in need of such treatment an effective amount of a compound of Formula (II):
- wherein:
- each of R1, R2, R3, R4, R5, R6, R7, R8 R9, R10, R11, R12, R13, R14, R15 R16, and R17 is independently selected from the group consisting of deuterium, hydrogen, alkyl, and deuteroalkyl;
- R18 is independently selected from the group consisting of hydrogen, deuterium, alkyl, deuteroalkyl, sodium, and potassium;
- or
- N-oxides, pharmaceutically acceptable salts, prodrugs, formulations, polymorphs, tautomers, racemic mixtures or stereoisomers thereof.
A method of treating an MMP mediated disease, comprising administering to a subject in need of such treatment an effective amount of a compound of Formula (II):
- wherein:
- each of R1, R2, R3, R4, R5, R6, R7, R8 R9, R10, R11, R12, R13, R14, R15 R16, and R17 is independently selected from the group consisting of deuterium, hydrogen, alkyl, hydroxyl and deuteroalkyl;
- R18 is independently selected from the group consisting of hydrogen, deuterium, alkyl, deuteroalkyl, sodium, and potassium;
- or
- N-oxides, pharmaceutically acceptable salts, prodrugs, formulations, polymorphs, tautomers, racemic mixtures or stereoisomers thereof.
(canceled)
(canceled)
A pharmaceutical composition comprising:
- A) an effective amount of a compound of Formula (II):
- wherein:
- each of R1, R2, R3, R4, R5, R6, R7, R8 R9, R10, R11, R12, R13, R14, R15 R16, and R17 is independently selected from the group consisting of deuterium, hydrogen, alkyl, hydroxyl and deuteroalkyl;
- R18 is independently selected from the group consisting of hydrogen, deuterium, alkyl, deuteroalkyl, sodium, and potassium;
- or
- N-oxides, pharmaceutically acceptable salts, prodrugs, formulations, polymorphs, tautomers, racemic mixtures or stereoisomers thereof;
- B) a pharmaceutically acceptable carrier;
- and
- C) a member selected from the group consisting of:
- (a) a disease modifying antirheumatic drug;
- (b) a nonsteroidal anti-inflammatory drug;
- (c) a COX-2 selective inhibitor;
- (d) a COX-1 inhibitor;
- (e) an immunosuppressive;
- (f) a steroid;
- (g) a biological response modifier;
- and (h) a small molecule inhibitor of pro-inflammatory cytokine production.
Dependencies are inferred from the claim text.