IP Library › Granted Patent US 11,746,095
Granted Patent B2
US 11,746,095 · App. 17/738,327 · Granted Sep 5, 2023

Inhibtors of RAF kinases

Inventors: Stephen W. Kaldor (San Diego, CA); Toufike Kanouni (Rancho Santa Fe, CA); Eric Murphy (San Marcos, CA); Jason Cox (Rancho Santa Fe, CA); Robert Kania (Del Mar, CA)
Assignee: KINNATE BIOPHARMA INC.
C07D295/155C07D401/12C07D405/12
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Quick Facts
Patent No.
US 11,746,095
App. No.
17/738,327
Granted
Sep 5, 2023
Kind
B2
Abstract

Provided herein are inhibitors of receptor tyrosine kinase effector, RAF, pharmaceutical compositions comprising said compounds, and methods for using said compounds for the treatment of diseases.

Claims (28)

1. A compound, or pharmaceutically acceptable salt or solvate thereof, selected from the group consisting of:

N-(3-[2-[(3R)-3-hydroxybut-1-yn-1-yl]-6-(morpholin-4-yl)pyridin-4-yl]-4-methylphenyl)-2-(trifluoromethyl)pyridine-4-carboxamide;

N-(3-[2-[(3S)-3-hydroxybut-1-yn-1-yl]-6-(morpholin-4-yl)pyridin-4-yl]-4-methylphenyl)-2-(trifluoromethyl)pyridine-4-carboxamide;

N-[3-[2-(3-hydroxy-3-methylbut-1-yn-1-yl)-6-(morpholin-4-yl)pyridin-4-yl]-4-methylphenyl]-2-(trifluoromethyl)pyridine-4-carboxamide;

N-[3-[2-(3-hydroxyprop-1-yn-1-yl)-6-(morpholin-4-yl)pyridin-4-yl]-4-methylphenyl]-2-(trifluoromethyl)pyridine-4-carboxamide;

(3S)—N-[3-[2-(2-aminopyrimidin-4-yl)-6-(morpholin-4-yl)pyridin-4-yl]-4-methylphenyl]-3-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide;

N-(3-{2-[(3S)-3-aminobut-1-yn-1-yl]-6-(morpholin-4-yl)pyridin-4-yl}-4-methylphenyl)-2-(trifluoromethyl)pyridine-4-carboxamide;

N-(3-{2-[(3R)-3-aminobut-1-yn-1-yl]-6-(morpholin-4-yl)pyridin-4-yl}-4-methylphenyl)-2-(trifluoromethyl)pyridine-4-carboxamide;

N-(3-{2-[3-(dimethylamino)prop-1-yn-1-yl]-6-(morpholin-4-yl)pyridin-4-yl}-4-methylphenyl)-2-(trifluoromethyl)pyridine-4-carboxamide;

N-{4-methyl-3-[2-(morpholin-4-yl)-6-[3-(pyrrolidin-1-yl)prop-1-yn-1-yl]pyridin-4-yl]phenyl}-2-(trifluoromethyl)pyridine-4-carboxamide;

N-(4-methyl-3-{2-[3-(methylamino)prop-1-yn-1-yl]-6-(morpholin-4-yl)pyridin-4-yl}phenyl)-2-(trifluoromethyl)pyridine-4-carboxamide;

N-(3-{2-[(3S)-3-aminobut-1-yn-1-yl]-6-(morpholin-4-yl)pyridin-4-yl}-4-methylphenyl)-2-(trifluoromethyl)pyridine-4-carboxamide;

N-(4-methyl-3-{2-[(3R)-3-(methylamino)but-1-yn-1-yl]-6-(morpholin-4-yl)pyridin-4-yl}phenyl)-2-(trifluoromethyl)pyridine-4-carboxamide;

N-[3-[2-(3-hydroxyprop-1-yn-1-yl)-6-(morpholin-4-yl)pyridin-4-yl]-4-methylphenyl]-2-(trifluoromethyl)pyridine-4-carboxamide;

N-(3-{2-[(3S)-3-aminobut-1-yn-1-yl]-6-(morpholin-4-yl)pyridin-4-yl}-4-methylphenyl)-2-(trifluoromethyl)pyridine-4-carboxamide;

N-{4-methyl-3-[2-(morpholin-4-yl)-6-[(3S)-4,4,4-trifluoro-3-hydroxybut-1-yn-1-yl)pyridin-4-yl]phenyl}-2-(trifluoromethyl)pyridine-4-carboxamide;

N-{4-methyl-3-[2-(morpholin-4-yl)-6-[(3R)-4,4,4-trifluoro-3-hydroxybut-1-yn-1-yl]pyridin-4-yl]phenyl}-2-(trifluoromethyl)pyridine-4-carboxamide;

N-{3-[2-(3-amino-3-methylbut-1-yn-1-yl)-6-(morpholin-4-yl)pyridin-4-yl]-4-methylphenyl}-2-(trifluoromethyl)pyridine-4-carboxamide; and

N-(3-{2-[(3S)-3-aminobut-1-yn-1-yl]-6-(morpholin-4-yl)pyridin-4-yl}-4-methylphenyl)-2-(trifluoromethyl)pyridine-4-carboxamide.

2. The compound, or pharmaceutically acceptable salt or solvate thereof, of claim 1 having the structure of: N-[3-[2-(3-hydroxy-3-methylbut-1-yn-1-yl)-6-(morpholin-4-yl)pyridin-4-yl]-4-methylphenyl]-2-(trifluoromethyl)pyridine-4-carboxamide.

3. The compound, or pharmaceutically acceptable salt or solvate thereof, of claim 1 having the structure of: N-{3-[2-(3-amino-3-methylbut-1-yn-1-yl)-6-(morpholin-4-yl)pyridin-4-yl]-4-methylphenyl}-2-(trifluoromethyl)pyridine-4-carboxamide.

4. The compound, or pharmaceutically acceptable salt or solvate thereof, of claim 1 having the structure of: N-(3-{2-[(3S)-3-aminobut-1-yn-1-yl]-6-(morpholin-4-yl)pyridin-4-yl}-4-methylphenyl)-2-(trifluoromethyl)pyridine-4-carboxamide.

5. The compound, or pharmaceutically acceptable salt or solvate thereof, of claim 1 having the structure of: N-(3-{2-[(3S)-3-aminobut-1-yn-1-yl]-6-(morpholin-4-yl)pyridin-4-yl}-4-methylphenyl)-2-(trifluoromethyl)pyridine-4-carboxamide.

6. A pharmaceutical composition comprising a compound, or pharmaceutically acceptable salt or solvate thereof, as described in claim 1 and a pharmaceutically acceptable excipient.

7. The pharmaceutical composition of claim 6 , wherein the compound is N-[3-[2-(3-hydroxy-3-methylbut-1-yn-1-yl)-6-(morpholin-4-yl)pyridin-4-yl]-4-methylphenyl]-2-(trifluoromethyl)pyridine-4-carboxamide, or pharmaceutically acceptable salt or solvate thereof.

8. The pharmaceutical composition of claim 6 , wherein the compound is N-{3-[2-(3-amino-3-methylbut-1-yn-1-yl)-6-(morpholin-4-yl)pyridin-4-yl]-4-methylphenyl}-2-(trifluoromethyl)pyridine-4-carboxamide, or pharmaceutically acceptable salt or solvate thereof.

9. The pharmaceutical composition of claim 6 , wherein the compound is N-(3-{2-[(3S)-3-aminobut-1-yn-1-yl]-6-(morpholin-4-yl)pyridin-4-yl}-4-methylphenyl)-2-(trifluoromethyl)pyridine-4-carboxamide, or pharmaceutically acceptable salt or solvate thereof.

10. The pharmaceutical composition of claim 6 , wherein the compound is N-(3-{2-[(3S)-3-aminobut-1-yn-1-yl]-6-(morpholin-4-yl)pyridin-4-yl}-4-methylphenyl)-2-(trifluoromethyl)pyridine-4-carboxamide, or pharmaceutically acceptable salt or solvate thereof.

Assignments (3)
CORRECTIVE ASSIGNMENT TO CORRECT THE CORRECT THE RECEIVING PARTY DATA COMPANY NAME IS: PIERRE FABRE MEDICAMENT PREVIOUSLY RECORDED AT REEL: 66638 FRAME: 147. ASSIGNOR(S) HEREBY CONFIRMS THE ASSIGNMENT. Recorded Sep 11, 2024
From: KINNATE BIOPHARMA INC.
To: PIERRE FABRE MÉDICAMENT
Reel/Frame 068939/0656 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 4, 2024
From: KINNATE BIOPHARMA INC.
To: PIERRE FABRE MÉDICAMENT, SAS
Reel/Frame 066638/0147 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 14, 2022
From: KALDOR, STEPHEN W.; KANOUNI, TOUFIKE; MURPHY, ERIC; COX, JASON; KANIA, ROBERT
To: KINNATE BIOPHARMA INC.
Reel/Frame 059907/0068 →
Continuity (3)
Continuation 17498530 · Oct 11, 2021
Provisional Application 63090623 · Oct 12, 2020
Related Publication 20220356160A1 · Nov 10, 2022
Cited By (2)
US 12,569,496 US 12,692,248