US 8,524,778 B2Granted

Biphenyl-4-yl-sulfonic acid arylamides and their use as therapeutic agents

AssigneePIMCO 2664 Limited

InventorsIain Robert Greig, Robert Jurgen Van't Hof, Stuart Hamilton Ralston

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Abstract

The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain aryl sulfonamides and related compounds (collectively referred to herein as ‘BPSAAA compounds’), as described herein, and including, for example, biphenyl-4-sulfonic acid (hydroxyalkyl-phenyl)-amides and related compounds. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, in treatment and/or prevention, for example, of inflammation and/or joint destruction and/or bone loss; of disorders mediated by excessive and/or inappropriate and/or prolonged activation of the immune system; of, inflammatory and autoimmune disorders, for example, rheumatoid arthritis, psoriasis, psoriatic arthritis, chronic obstructive pulmonary disease (COPD), atherosclerosis, inflammatory bowel disease, ankylosing spondylitis, and the like; of disorders associated with bone loss, such as bone loss associated with excessive osteoclast activation in rheumatoid arthritis, osteoporosis, cancer associated bone disease, Paget's disease and the like.

Claims50

Dependent claims

A compound selected from compounds of the following formula and pharmaceutically acceptable salts thereof:

wherein:
Ar1—Ar2— is a group of the following formula:
q is independently 0, 1, or 2;
r is independently 0, 1, 2, or 3;
each RP is independently a ring substituent;
—RN is independently —H or —RNN;
—RNN is C1-6alkyl;
—Ar3— is independently 1,3-phenylene or 1,4-phenylene, and is optionally substituted with one or more substituents —RAR3, wherein each —RAR3 is independently a ring substituent;
—Z is independently —OH or —O—W;
-J- is —Ralk—;
—Ralk— is saturated aliphatic C1-5alkylene, and is optionally substituted with one or more substituents —RAA, wherein each —RAA is independently —F, —Cl, —Br, —I, —OH,
—ORA2, —OCF3, —NH2, —NHRA2, —NRA22, —C(═O)NH2, —C(═O)NHRA2, or —C(═O)NRA22, wherein each RA2 is independently C1-4alkyl;
—W is independently —RE1, —C(═O)—RE2, or —C(═O)—O—RE3;
each of RE1, RE2, and RE3 is independently —H, C1-3alkyl, phenyl, or —CH2-phenyl;
and
each ring substituent is independently —F, —Cl, —Br, —I, —RD9, —CF3, —OH, —ORD9, —OCF3, —CN, —NO2, —NH2, —NHRD9, or —NRD92, wherein each —RD9 is independently saturated aliphatic C1-3alkyl.

13 more elements

Dependencies are inferred from the claim text.

Facts

Application: 12/531,732Filed 20 Mar 2008
Priority: GB 0705400.021 Mar 2007
Published: US 2010/0286266 A111 Nov 2010
Granted: 3 Sep 2013
Term ends: Not estimatedThe source records don’t support an estimate.

Classification20 codes

C07C 311/21
Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings: having the nitrogen atom of at least…
A61P 1/04
Drugs for disorders of the alimentary tract or the digestive system: for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of…
A61P 3/14
For electrolyte homeostasis: for calcium homeostasis
A61P 9/10
Drugs for disorders of the cardiovascular system: for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary…