METHOD OF USE FOR SUBSTITUTED DIPIPERIDINE CCR2 ANTAGONISTS

Abstract

The present invention is directed to a method for use of substituted dipiperidine compounds of Formula (I)

Description

Claims

1. A method for treating a subject having a syndrome, disorder or disease related to CCR2 activation, said method comprising administering to said subject an effective amount of a compound of Formula (I):

2. The method of claim 1, wherein the compound of claim 1 is (S)-{[4-(1H-indol-3-yl)-piperidin-1-yl]}-{1-[(2E)-3-(3,4,5-triflouro-phenyl)-acryloyl]-piperidin-4-yl}-acetic acid or a salt, isomer, prodrug, metabolite or polymorph thereof.

3. The method of claim 3, wherein the compound of claim 1 is (S)-{[4-(1H-indol-3-yl)-piperidin-1-yl]}-{1-[(2E)-3-(3,4,5-trifluoro-phenyl)-acryloyl]-piperidin-4-yl}-acetic acid or a salt, isomer, prodrug, metabolite or polymorph thereof.

4. The method of claim 3, wherein the compound of claim 1 is (S)-{[4-(1H-indol-3-yl)-piperidin-1-yl]}-{1-[(2E)-3-(3,4,5-trifluoro-phenyl)-acryloyl]piperidin-4-yl}-acetic acid or a salt, isomer, prodrug, metabolite or polymorph thereof.

5. The method of claim 3, wherein the syndrome, disorder or disease is selected from ophthalmic disorders, uveitis, atherosclerosis, rheumatoid arthritis, psoriasis, psoriatic arthritis, atopic dermatitis, multiple sclerosis, Crohn's Disease, ulcerative colitis, nephritis, organ allograft rejection, fibroid lung, renal insufficiency, Type II diabetes and diabetic complications, diabetic nephropathy, diabetic retinopathy, diabetic retinitis, diabetic microangiopathy, obesity, tuberculosis, chronic obstructive pulmonary disease, sarcoidosis, invasive staphyloccocia, inflammation after cataract surgery, allergic rhinitis, allergic conjunctivitis, chronic urticaria, asthma, allergic asthma, periodontal diseases, periodonitis, gingivitis, gum disease, diastolic cardiomyopathies, cardiac infarction, myocarditis, chronic heart failure, angiostenosis, restenosis, reperfusion disorders, glomerulonephritis, solid tumors and cancers, chronic lymphocytic leukemia, chronic myelocytic leukemia, multiple myeloma, malignant myeloma, Hodgkin's disease, and carcinomas of the bladder, breast, cervix, colon, lung, prostate, or stomach.

6. The method of claim 3, wherein the effective amount is from about 0.1 ng/kg/day to about 300 mg/kg/day.

7. The method of claim 5, wherein the syndrome, disorder or disease is obesity.

8. The method of claim 3, wherein the effective amount reduces weight gain and body fat mass gain.

9. The method of claim 7, wherein the syndrome, disorder or disease is selected from Type II diabetes and diabetic complications.

10. The method of claim 9, wherein diabetic complications are selected from diabetic nephropathy, diabetic retinopathy, diabetic retinitis or diabetic microangiopathy.

11. The method of claim 10, wherein the effective amount increases insulin sensitivity.

12. The method of claim 5, wherein the compound of claim 1 is administered in combination with one or more other therapeutic agents.

13. The method of claim 12, wherein the other therapeutic agent is one or more anti-inflammatory agents is selected from an antibiotic, corticosteroid or steroid anti-infective agent or immunosuppressive agent.