Long chain base sphingosine kinase inhibitors

Patent metadata

Field	Value
Publication number	US-9688668-B2
Application number	US-201314377300-A
Country	US
Kind code	B2
Filing date	Feb 8, 2013
Priority date	Feb 8, 2012
Publication date	Jun 27, 2017
Grant date	Jun 27, 2017

Abstract

The invention relates to inhibitors of Sphingosine Kinase enzymatic activity, and methods of treating diseases and disorders by administering inhibitors of Sphingosine Kinase enzymatic activity.

First claim

The claimed invention is:

1. A compound that is selected from the group consisting of:

and pharmaceutically acceptable salts thereof.

2. A compound that is selected from the group consisting of:

and pharmaceutically acceptable salts thereof.

3. A pharmaceutical composition comprising the compound of claim 1 or 2 , and a pharmaceutically acceptable carrier.

4. A method for the treatment of a pathological condition or symptom in a mammal, wherein inhibition of the SphK1 enzyme or SphK2 enzyme, or both SphK1 and SphK2 enzymes is implicated and such inhibition is desired, comprising administering to said mammal an effective amount of the compound of claim 1 or 2 .

5. The method of claim 4 , wherein the pathological condition comprises age-related macular degeneration or diabetic retinopathy;
a hyperproliferative disorder;
cancer;
a hypertensive disease or disorder;
or an inflammatory disease or disorder, or fibrosis.

6. The method of claim 5 , wherein the inflammatory disease or disorder is an inflammatory kidney disease selected from the group consisting of glomerulonephritis, glomerular injury, nephrotic syndrome, interstitial nephritis, lupus nephritis, Goodpasture's disease, Wegener's granulomatosis, renal vasculitis, IgA nephropathy, diabetic nephropathy, chronic allograft nephropathy and idiopathic glomerular disease.

Assignees

• Univ Virginia Patent Foundation

Inventors

• Santos Webster L
• Lynch Kevin R
• Macdonald Timothy L
• Kennedy Andrew
• Kharel Yugesh
• Raje Mithun Rajendra
• Houck Joseph

Classifications

• A61P35/00

  Antineoplastic agents · CPC title

• C07D271/06

  1,2,4-Oxadiazoles; Hydrogenated 1,2,4-oxadiazoles · CPC title

• C07C279/00

  Derivatives of guanidine, i.e. compounds containing the group [IMAGE cpc-sch-C07C-0970.gif], the singly-bound nitrogen atoms not being part of nitro or nitroso groups · CPC title

• C07C251/12

  being acyclic · CPC title

• C07D413/04 Primary

  directly linked by a ring-member-to-ring-member bond · CPC title