IP Library Granted Patent US 8,969,565
Granted Patent B2
US 8,969,565 · App. 13/785,271 · Granted Mar 3, 2015

Imidazo[1,2-b]pyridazine-based compounds, compositions comprising them, and methods of their use

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Quick Facts
Patent No.
US 8,969,565
App. No.
13/785,271
Granted
Mar 3, 2015
Kind
B2
Abstract

Imidazo[1,2-b]pyridazine-based compounds of the formula: are disclosed, wherein R 1 , R 2 and R 3 are defined herein. Compositions comprising the compounds and methods of their use to treat, manage and/or prevent diseases and disorders mediated by mediated by adaptor associated kinase 1 activity are also disclosed.

Claims (28)

1. A compound of the formula:

or a pharmaceutically acceptable salt thereof, wherein:

each R 1A is independently —OR 1C , —N(R 1C ) 2 , —C(O)R 1C , —C(O)OR 1C , —C(O)N(R 1C ) 2 , —N(R 1C )C(O)OR 1C , cyano, halo, or optionally substituted C 1-12 hydrocarbyl or 2-12-membered heterocarbyl, which optional substitution is with one or more R 1B ;

each R 1B is independently —OR 1C , —N(R 1C ) 2 , —C(O)R 1C , —C(O)OR 1C , —C(O)N(R 1C ) 2 , —N(R 1C )C(O)OR 1C , cyano or halo;

each R 1C is independently hydrogen or optionally substituted C 1-12 hydrocarbyl or 2-12-membered heterocarbyl, which optional substitution is with one or more of cyano, halo or hydroxyl;

each R 2C is independently —OR 2D , —N(R 2D ) 2 , —C(O)R 2D , —C(O)N(R 2D ) 2 , —N(R 2D )C(O)OR 2D , cyano, halo, or optionally substituted C 1-12 hydrocarbyl or 2-12-membered heterocarbyl, which optional substitution is with one or more with one or more amino, cyano, halo, hydroxyl, or R 2D ;

each R 2D is independently hydrogen or optionally substituted C 1-12 hydrocarbyl or 2-12-membered heterocarbyl, which optional substitution is with one or more of amino, cyano, halo, hydroxyl; and

m is 0-3.

2. The compound of claim 1 , which is of the formula:

3. The compound of claim 1 , which is of the formula:

4. A compound of the formula:

or a pharmaceutically acceptable salt thereof, wherein:

X is CH or N;

each R 1A is independently —OR 1C , —N(R 1C ) 2 , —C(O)R 1C , —C(O)OR 1C , —C(O)N(R 1C ) 2 , —N(R 1C )C(O)OR 1C , cyano, halo, or optionally substituted C 1-12 hydrocarbyl or 2-12-membered heterocarbyl, which optional substitution is with one or more R 1B ;

each R 1B is independently —OR 1C , —N(R 1C ) 2 , C(O)R 1C , —C(O)OR 1C , —C(O)N(R 1C ) 2 , —N(R 1C )C(O)OR 1C , cyano or halo;

each R 1C is independently hydrogen or optionally substituted C 1-12 hydrocarbyl or 2-12-membered heterocarbyl, which optional substitution is with one or more of cyano, halo or hydroxyl;

each R 2C is independently —C(O)OR 2D , —C(O)N(R 2D ) 2 , or —N(R 2D )C(O)OR 2D , which optional substitution is with one or more with one or more amino, cyano, halo, hydroxyl, or R 2D ;

R 2D is 2-12-membered heterocarbyl comprising at least one nitrogen atom; and

m is 0-3.

5. A compound of the formula:

or a pharmaceutically acceptable salt thereof, wherein:

X is CH or N;

each R 1A is independently —OR 1C , —N(R 1C ) 2 , —C(O)R 1C , —C(O)OR 1C , —C(O)N(R 1C ) 2 , —N(R 1C )C(O)OR 1C , cyano, halo, or optionally substituted C 1-12 hydrocarbyl or 2-12-membered heterocarbyl, which optional substitution is with one or more R 1B ;

each R 1B is independently —OR 1C , —N(R 1C ) 2 , —C(O)R 1C , —C(O)OR 1C , —C(O)N(R 1C ) 2 , —N(R 1C )C(O)OR 1C , cyano or halo;

each R 1C is independently hydrogen or optionally substituted C 1-12 hydrocarbyl or 2-12-membered heterocarbyl, which optional substitution is with one or more of cyano, halo or hydroxyl;

each R 2C is independently —C(O)R 2D ;

each R 2D is 2-12-membered heterocarbyl comprising at least one nitrogen atom; and

m is 0-3.

Assignments (6)
RELEASE OF SECURITY INTEREST Recorded May 5, 2026
From: OXFORD FINANCE LLC
To: LEXICON PHARMACEUTICALS, INC.; LEXICON PHARMACEUTICALS
Reel/Frame 075545/0601 →
SECURITY INTEREST Recorded May 4, 2026
From: LEXICON PHARMACEUTICALS, INC.; LEXICON PHARMACEUTICALS (NEW JERSEY), INC.; LION ACQUISITION CORPORATION
To: HERCULES CAPITAL, INC., AS AGENT
Reel/Frame 075498/0899 →
SECURITY INTEREST Recorded Mar 17, 2022
From: LEXICON PHARMACEUTICALS, INC.
To: OXFORD FINANCE LLC, AS COLLATERAL AGENT
Reel/Frame 059432/0709 →
RELEASE OF SECURITY INTEREST Recorded Sep 14, 2020
From: BIOPHARMA CREDIT PLC
To: LEXICON PHARMACEUTICALS, INC.
Reel/Frame 053767/0445 →
SECURITY INTEREST Recorded Dec 20, 2017
From: LEXICON PHARMACEUTICALS, INC.
To: BIOPHARMA CREDIT PLC
Reel/Frame 044958/0377 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 3, 2013
From: BI, YINGZHI; CARSON, KENNETH GORDON; CIANCHETTA, GIOVANNI; GREEN, MICHAEL ALAN; KUMI, GODWIN; LIANG, ZHI; LIU, YING JADE; MAIN, ALAN; ZHANG, YULIAN; ZIPP, GLENN GREGORY
To: LEXICON PHARMACEUTICALS, INC.
Reel/Frame 030344/0188 →