Diazole lactams

Patent metadata

Field	Value
Publication number	US-2016303084-A1
Application number	US-201615074976-A
Country	US
Kind code	A1
Filing date	Mar 18, 2016
Priority date	Dec 7, 2012
Publication date	Oct 20, 2016
Grant date	—

Abstract

Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are diazole lactam derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated disease, and as controls in assays for the identification of competitive CCR1 antagonists.

First claim

1 .- 21 . (canceled)

22 . A method of treating CCR1-mediated diseases or conditions comprising administering to a subject in need thereof a therapeutically effective amount of a compound selected from the group consisting of:

or a pharmaceutically acceptable salt, hydrate, solvate, rotamer or N-oxide thereof.

23 . A method in accordance with claim 22 , wherein said CCR1-mediated disease or condition is an inflammatory condition.

24 . A method in accordance with claim 22 , wherein said CCR1-mediated disease or condition is an immunoregulatory disorder.

25 . A method in accordance with claim 22 , wherein said CCR1-mediated disease or condition is selected from the group consisting of transplant rejection, dermatitis, eczema, urticaria, vasculitis, inflammatory bowel disease, food allergy, asthma, Alzheimer's disease, Parkinson's disease, psoriasis, lupus erythematosus, stroke, restenosis and encephalomyelitis.

26 . A method in accordance with claim 22 , wherein said CCR1-mediated disease or condition is selected from the group consisting of rheumatoid arthritis, multiple sclerosis, osteoarthritis, multiple myeloma and osteoporosis.

27 . A method in accordance with claim 22 , wherein said administering is oral, parenteral, rectal, transdermal, sublingual, nasal or topical.

28 . A method in accordance with claim 22 , wherein said compound is administered in combination with an anti-inflammatory agent, analgesic agent, an anti-proliferative agent, a metabolic inhibitor, a leukocyte migration inhibitor or an immuno modulator.

29 . A method in accordance with claim 22 , wherein said compound is selected from the group consisting of

or a pharmaceutically acceptable salt, hydrate, solvate, rotamer or N-oxide thereof.

30 . A method in accordance with claim 22 , wherein said compound is selected from the group consisting of

or a pharmaceutically acceptable salt, hydrate, solvate, rotamer or N-oxide thereof.

31 . A method in accordance with claim 22 , wherein said compound is

or a pharmaceutically acceptable salt, hydrate, solvate, rotamer or N-oxide thereof.

32 . A method in accordance with claim 22 , wherein said compound is

or a pharmaceutically acceptable salt, hydrate, solvate, rotamer or N-oxide thereof.

Assignees

• Chemocentryx Inc

Inventors

• Chen Xi
• Fan Pingchen
• Li Yandong
• Powers Jay P
• Malathong Viengkham
• Punna Sreenivas
• Tanaka Hiroko
• Zhang Penglie

Classifications

• A61P37/08

  Antiallergic agents (antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14) · CPC title

• A61P9/14

  Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers · CPC title

• A61P9/10

  for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis · CPC title

• A61P37/06

  Immunosuppressants, e.g. drugs for graft rejection · CPC title

• A61P43/00

  Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title