IP Library › Granted Patent US 10,709,712
Granted Patent B2
US 10,709,712 · App. 16/274,165 · Granted Jul 14, 2020

Biaryl amide compounds as kinase inhibitors

Inventors: Robert John Aversa (Cambridge, MA); Paul Andrew Barsanti (Pleasant Hill, CA); Matthew T. Burger (Cambridge, MA); Michael Patrick Dillon (Castro Valley, CA); Alan Dipesa (Boston, MA); Cheng Hu (San Mateo, CA); Yan Lou (Pleasanton, CA); Gisele A. Nishiguchi (Arlington, MA); Yue Pan (Lexington, MA); Valery Rostislavovich Polyakov (Moraga, CA); Savithri Ramurthy (Walnut Creek, CA); Alice C. Rico (Castro Valley, CA); Lina Quattrocchio Setti (Fremont, CA); Aaron Smith (Fremont, CA); Sharadha Subramanian (San Ramon, CA); Benjamin R. Taft (Emeryville, CA); Huw Roland Tanner (San Francisco, CA); Lifeng Wan (Emeryville, CA); Naeem Yusuff (Cambridge, MA)
Assignee: NOVARTIS AG
A61K31/5377A61K31/444A61K31/501A61K31/5375A61K31/541A61K45/06C07B59/002C07D213/74C07D213/75C07D213/81C07D213/82C07D213/84C07D233/88C07D237/20C07D237/22C07D237/24C07D239/42C07D239/47C07D239/48C07D241/20C07D263/58C07D277/42C07D401/04C07D401/12C07D401/14C07D403/04C07D403/12C07D405/04C07D405/12C07D405/14C07D409/14C07D413/04C07D413/12C07D413/14C07D417/12C07D471/04C07D487/04C07D491/04C07D491/048C07D491/08C07D491/107C07D493/04C07D493/10C07D495/04C07D498/08C07D513/04C07B2200/05
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Quick Facts
Patent No.
US 10,709,712
App. No.
16/274,165
Granted
Jul 14, 2020
Kind
B2
Abstract

The present invention provides compounds of Formula (I) as described herein, and salts thereof, and therapeutic uses of these compounds for treatment of disorders associated with Raf kinase activity. The invention further provides pharmaceutical compositions comprising these compounds, and compositions comprising these compounds and a therapeutic co-agent.

Claims (9)

1. A method of treating a proliferative disease mediated by B-Raf or C-Raf in a patient having said disease, comprising administering to a patient in need thereof a therapeutically effective amount of a compound which is

or a pharmaceutically acceptable salt thereof.

2. The method of claim 1 wherein the proliferative disease is a cancer selected from solid tumors, melanoma, breast cancer, non-small cell lung cancer, lung adenocarcinoma, sarcoma, gastrointestinal stromal tumors, ovarian cancer, colorectal cancer, thyroid cancer and pancreatic cancer.

3. The method of claim 2 wherein the proliferative disease is melanoma.

4. A method of treating a proliferative disease mediated by B-Raf or C-Raf in a patient having said disease, comprising administering to a patient in need thereof a therapeutically effective amount of a compound which is

or a pharmaceutically acceptable salt thereof, in combination with one or more therapeutically active co-agents.

5. The method of claim 4 wherein the one or more therapeutically active co-agents is a RAF pathway inhibitor selected from paclitaxel, docetaxel, temozolomide, platins, doxorubicins, vinblastins, cyclophosphamide, topotecan, gemcitabine, ifosfamide, etoposide and irinotecan.

6. The method of claim 5 wherein the proliferative disease is a cancer selected from solid tumors, melanoma, breast cancer, non-small cell lung cancer, lung adenocarcinoma, sarcoma, gastrointestinal stromal tumors, ovarian cancer, colorectal cancer, thyroid cancer and pancreatic cancer.

7. The method of claim 6 wherein the proliferative disease is melanoma.

Assignments (6)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 21, 2019
From: AVERSA, ROBERT; BARSANTI, PAUL A.; BURGER, MATTHEW; DILLON, MICHAEL PATRICK; HU, CHENG; LOU, YAN; NISHIGUCHI, GISELE; PAN, YUE; POLYAKOV, VALERY; RAMURTHY, SAVRITHI; RICO, ALICE; SETTI, LINA; SMITH, AARON; SUBRAMANIAN, SHARADHA; TAFT, BENJAMIN; TANNER, HUW; WAN, LIFENG
To: NOVARTIS VACCINES AND DIAGNOSTICS, INC.
Reel/Frame 048393/0490 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 21, 2019
From: NOVARTIS VACCINES AND DIAGNOSTICS, INC.
To: NOVARTIS AG
Reel/Frame 048393/0525 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 21, 2019
From: YUSUFF, NAEEM
To: NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH INC.
Reel/Frame 048393/0561 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 21, 2019
From: NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH INC.
To: NOVARTIS AG
Reel/Frame 048393/0650 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 21, 2019
From: DIPESA, ALAN
To: NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH INC.
Reel/Frame 048393/0684 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 21, 2019
From: NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH INC.
To: NOVARTIS AG
Reel/Frame 048393/0724 →
Continuity (4)
Division 15601423 · May 22, 2017
Division 14774431
Provisional Application 61783558 · Mar 14, 2013
Related Publication 20190175606A1 · Jun 13, 2019
Cited By (1)
US 12,187,703