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NZ783053B2 - Polycyclic tlr7/8 antagonists and use thereof in the treatment of immune disorders - Google Patents
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NZ783053B2 - Polycyclic tlr7/8 antagonists and use thereof in the treatment of immune disorders - Google Patents

Polycyclic tlr7/8 antagonists and use thereof in the treatment of immune disorders Download PDF

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Publication number
NZ783053B2
NZ783053B2 NZ783053A NZ78305316A NZ783053B2 NZ 783053 B2 NZ783053 B2 NZ 783053B2 NZ 783053 A NZ783053 A NZ 783053A NZ 78305316 A NZ78305316 A NZ 78305316A NZ 783053 B2 NZ783053 B2 NZ 783053B2
Authority
NZ
New Zealand
Prior art keywords
compound
ghmatters
chemical structure
tlr7
ring
Prior art date
Application number
NZ783053A
Other versions
NZ783053A (en
Inventor
Nadia Brugger
Brian A Sherer
Original Assignee
Merck Patent Gmbh
Filing date
Publication date
Application filed by Merck Patent Gmbh filed Critical Merck Patent Gmbh
Publication of NZ783053A publication Critical patent/NZ783053A/en
Publication of NZ783053B2 publication Critical patent/NZ783053B2/en

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Abstract

The present invention relates to compounds of Formula (I), compositions comprising said compounds, and uses of said compounds. In Formula (I), Ring A is phenyl, pyridyl or pyrimidinyl; Ring B is pyridyl, pyrimidinyl, pyrazinyl, or pyrazolyl; and X is C(R4)2, with one R4 being H and the other R4 being an N-substituted amide group attached to the carbon at the carboxy group of the amide. Such compounds are useful as toll-like receptor 7/8 (TLR7/8) antagonists, and are able to treat a range of TLR7/8-mediated disorders such as arthritis.

Claims (8)

1. A compound of formula I, or a ceutically acceptable salt thereof, wherein: Ring A is , or ; Ring B is , , or ; R1 is -CF3 or –CN; R3 is hydrogen or C1-6 aliphatic; X is C(R4)2, with one R4 being -H and the other R4 being: 21072067_1 (GHMatters) P108799.NZ.2 , , , , , , , , O O , H , , , , or ; k is 0 or 1; n is 0; p is 0 or 1; r is 0; and t is 0.
2. The compound of claim 1, or a pharmaceutically able salt thereof, wherein Ring A 21072067_1 (GHMatters) P108799.NZ.2 , , or .
3. The compound of claim 1 or 2, or a pharmaceutically acceptable salt thereof, wherein Ring , , or .
4. The compound of claim 1, of formula I-h, or a pharmaceutically acceptable salt thereof.
5. The compound of claim 1, of formula I-J, 67_1 (GHMatters) P108799.NZ.2 or a ceutically acceptable salt thereof.
6. A compound, or a pharmaceutically acceptable salt thereof, selected from: Compound Example Chemical Structure Number Number 1 1 2 1 21072067_1 (GHMatters) P108799.NZ.2 Compound Example Chemical Structure Number Number 3 2 373 105 379 105 397 108 67_1 (GHMatters) P108799.NZ.2 Compound Example Chemical Structure Number Number 403 108 407 108 414 1 415 1 67_1 (GHMatters) P108799.NZ.2 nd Example Chemical Structure Number Number 416 1 419 1 420 1 421 1 N 21072067_1 (GHMatters) P108799.NZ.2 Compound Example Chemical Structure Number Number 422 1 427 1 432 105 433 1 67_1 (GHMatters) P108799.NZ.2 nd Example Chemical Structure Number Number 434 1 436 111 N F F 439 1 440 1 N 21072067_1 (GHMatters) P108799.NZ.2 nd Example Chemical Structure Number Number 441 111 442 111 N F F 444 113 N Isomer 1 F F 445 113 21072067_1 (GHMatters) P108799.NZ.2 Compound e Chemical Structure Number Number 446 111 453 118 463 118 464 120 21072067_1 (GHMatters) P108799.NZ.2
7. A pharmaceutical composition comprising a compound of any one of claims 1-6, and a pharmaceutically acceptable adjuvant, carrier, or vehicle.
8. Use of a compound of any one of claims 1-6, or a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for treating a TLR
NZ783053A 2016-12-16 Polycyclic tlr7/8 antagonists and use thereof in the treatment of immune disorders NZ783053B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562268765P 2015-12-17 2015-12-17
US201662353603P 2016-06-23 2016-06-23
NZ777345A NZ777345B2 (en) 2016-12-16 Polycyclic tlr7/8 antagonists and use thereof in the treatment of immune disorders

Publications (2)

Publication Number Publication Date
NZ783053A NZ783053A (en) 2024-08-30
NZ783053B2 true NZ783053B2 (en) 2024-12-03

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