Back to results
US 2017/0304255 A1Published application
Ppar agonists, compounds, pharmaceutical compositions, and methods of use thereof
AssigneesMitobridge, Inc., The Salk Institute for Biological Studies
InventorsThomas Baiga, Michael Downes, Ronald Evans, Arthur Kluge, Bharat Lagu, Masanori Miura, Sunil Kumar Panigrahi, Michael Patane, Susanta Samajdar, Ramesh Senaiar, Taisuke Takahashi
Life of this patent
Estimating the term…
Abstract
Provided herein are compounds of formula (I) useful for the treatment of PPAR-delta related diseases (e.g. mitochondrial diseases, muscular diseases, vascular diseases, demyelinating diseases and metabolic diseases).
Claims32
A compound of Formula (I):
- or a pharmaceutically acceptable salt thereof,
- wherein:
- Z is CH, N, or
- Ring A is optionally substituted phenylene when Z is CH, optionally substituted pyridinylene when Z is N, or optionally substituted N-oxide pyridinylene when Z is
- Ar is optionally substituted 5 or 6-membered monocyclic arylene or heteroarylene, provided that when Ar is 5-membered heteroarylene, R2 and —C(O)NR3— are oriented 1, 3 to each other on the ring, wherein position 1 is the point of attachment of Ar to the —C(O)NR3—;
- or
- Ar is optionally substituted 9- or 10-membered fused bicyclic heteroarylene;
- R1 is —OR1A or —NR1AR1B;
- R1A, R1B are each independently hydrogen or C1-C4-alkyl;
- W is O, and L is —(CH2)n—, wherein n is an integer between 1 and 6, and one or more (CH2) is replaced with —CH2—CH(CH3)—, —CH(CH3)—CH2—, —CH2—C(CH3)2—, —C(CH3)2—CH2—, —HC═C(CH3)—, —(CH3)C═CH—,
- —CH2—O—CH2—, —CH2—S—CH2—, —CH2—CH(F)—, —CH(F)—CH2—, —CH2—CF2—, —CF2—CH2—, —CH2—C(O)—, —C(O)—CH2—, optionally substituted arylene, optionally substituted arylene ether, or optionally substituted heteroarylene;
- or
- W is CH2, CH═CH, or C≡C, and L is —(CH2)n—, wherein n is an integer between 1 and 6, and one or more (CH2) is optionally replaced with —CH2—CH(CH3)—, —CH(CH3)—CH2—, —CH2—C(CH3)2—, —C(CH3)2—CH2—, —HC═C(CH3)—, —(CH3)C═CH—,
- —CH2—O—CH2—, —CH2—S—CH2—, —CH2—CH(F)—, —CH(F)—CH2—, —CH2—CF2—, —CF2—CH2—, —CH2—C(O)—, or —C(O)—CH2—;
- each R21 is independently hydrogen, halogen, or C1-C4-alkyl;
- R2 is halogen, C1-C4-alkyl, C3-C6-cycloalkyl, CN, C1-C4-alkoxy, C1-C4-haloalkoxy, SO2(C1-C4-alkyl), 5- or 6-membered heterocycloalkyl, —≡—R2A, —O(CH2)mR2B, NH(C1-C4-alkyl), N(C1-C4-alkyl)2, C(O)(C1-C4-alkyl), optionally substituted aryl, or optionally substituted 5-membered heteroaryl;
- m is an integer having an a value of 0, 1, 2, or 3;
- R2A and R2B are each independently C1-C4-alkyl, C3-C6-cycloalkyl, or C1-C4 haloalkyl;
- R3 is C1-C4-alkyl,
- or C1-C4-haloalkyl;
- and
- each R4 is independently H, D, or F;
- with the proviso that the compound is not selected from the group consisting of:
- or a pharmaceutically acceptable salt thereof.
21 more elements
4-5. (canceled)
(canceled)
9-10. (canceled)
12-13. (canceled)
16-17. (canceled)
20-21. (canceled)
(canceled)
(canceled)
31-35. (canceled)
38-39. (canceled)
42-49. (canceled)
Dependencies are inferred from the claim text.