S1P and/or ATX modulating agents

US9850206B2 · kind B2 · utility

Assignee

• Biogen MA Inc. · US

Inventors

• Hairuo Peng · Needham, US
• Edward Yin-Shiang Lin · Ashland, US
• Jianhua Chao · Pompton Lakes, US
• Zhili Xin · Lake Bluff, US
• Bin Ma · Arlington, US
• Kevin M. Guckian · Northborough, US
• Timothy Chan · Cambridge, US
• Gnanasambandam Kumaravel · Westford, US
• Arthur G. Taveras · Rockaway, US

Key dates

• Filing date: Nov 20, 2013
• Grant date: Dec 26, 2017
• Expiry date: Nov 20, 2033

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D403/04
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Compounds of formula (I) wherein: X is —O—, —S(O)r—, —CH2—, or —NR—, wherein r is 0, 1, or 2; X1, X2, and X5 are each independently CR7 or N; one of X3 or X4 is C and is attached by a single bond to -L-, and the other is CR7 or N, provided that no more than three of X1, X2, X3, X or X5 are N; Ring A is monocyclic C5-6scycloalkyl or a 5- to 6-membered monocyclic heterocyclyl comprising from 1 to 5 heteroatoms independently selected from N, S, or O; wherein Ring A is further optionally substituted with from 1 to 3 R4; provided that Ring A is not morpholinyl, thiomorpholinyl or tetrahydro-2H-pyranyl; L is a bond, —O—, —NR—, —S(O)n—, —CH2—, or —C(O)—, wherein n is 0, 1, or 2; 1 2 L1 is an C1-8alkylene, C3-scycloalkylene, —CH2-L2-, or a 3- to 8-membered heterocyclylene comprising 1 to 5; R1 is C6-20alkyl or a monocyclic C3-8cycloalkyl; wherein said C3-8cycloalkyl is substituted with at least one R6 and may be optionally substituted with from 1 to 5 additional R6 substituents, wherein R6 for each occurrence is independently selected; and R2 is —C(O)OR3, —C(O)N(R3)—S(O)2R3, —S(O)2OR3, —C(O)NHC(O)R3, —Si(O)OH, —B(OH)2, —N(R3)S(O)2R3, —S(O)2N(R3)2, —O—P(O)(OR3)2, or —P(O)(OR3)2, —CN, —S(O)2…