IP Library Granted Patent US 11,773,070
Granted Patent B2
US 11,773,070 · App. 17/865,236 · Granted Oct 3, 2023

Dihydrooxadiazinones

Inventors: Manuel Ellermann (Berlin, DE); Stefan Nikolaus Gradl (Berlin, DE); Charlotte Christine Kopitz (Falkenesee, DE); Martin Lange (Berlin, DE); Adrian Tersteegen (Wuppertal, DE); Philip Lienau (Berlin, DE); Christa Hegele-Hartung (Mülheim an der Ruhr, DE); Detlev Sülzle (Berlin, DE); Timothy A. Lewis (Cambridge, MA); Heidi Greulich (Cambridge, MA); Xiaoyun Wu (Cambridge, MA); Matthew Meyerson (Boston, MA); Alex Burgin (Cambridge, MA)
Assignees: Bayer Aktiengesellschaft; Bayer Pharma Aktiengesellschaft; The Broad Institute, Inc.; Dana-Farber Cancer Institute, Inc.
C07D273/04C07D413/10C07D413/12C07D417/10C07D471/04C07D491/107C07D495/10
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Quick Facts
Patent No.
US 11,773,070
App. No.
17/865,236
Granted
Oct 3, 2023
Kind
B2
Abstract

The present invention provides dihydrooxydiazinone compounds of general formula (I) in which R 1 , R 2 , R 3 , and R 4 , are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative diseases, as a sole agent or in combination with other active ingredients.

Claims (13)

1. A compound having the structure

(6S)-5-[4′-fluoro-2-(trifluoromethyl)biphenyl-4-yl]-6-methyl-3,6-dihydro-2H-1,3,4-oxadiazin-2-one,

or a stereoisomer, a tautomer, an N-oxide, a hydrate, a solvate, or a salt thereof, or a mixture of same.

2. A pharmaceutical composition comprising the compound of claim 1 and one or more pharmaceutically acceptable excipients.

3. A pharmaceutical combination comprising:

the compound of claim 1 , and

one or more further anti-cancer agents.

4. A method for the treatment of a disease sensitive to phosphodiesterase 3A (PDE3A) or phosphodiesterase 3B (PDE3B) modulation in a subject, comprising administering to the subject the compound of claim 1 .

5. The method according to claim 4 , wherein the disease is a hyperproliferative disease.

6. The method according to claim 5 , wherein the hyperproliferative disease is a cancer disease.

7. The method according to claim 6 , wherein the cancer disease is selected from brain cancer, breast cancer, cervical cancer, AML, lung cancer, skin cancer, esophageal carcinoma, ovarian cancer, pancreas cancer and prostate cancer.

8. The method according to claim 6 , wherein the cancer disease is selected from glioma, glioblastoma, and ovarian cancer.

9. The method according to claim 6 , wherein the cancer disease is melanoma.

Assignments (3)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 14, 2023
From: ELLERMANN, MANUEL; GRADL, STEFAN NIKOLAUS; KOPITZ, CHARLOTTE CHRISTINE; LANGE, MARTIN; TERSTEEGEN, ADRIAN; LIENAU, PHILIP; HEGELE-HARTUNG, CHRISTA; SÜLZLE, DETLEV
To: BAYER AKTIENGESELLSCHAFT; BAYER PHARMA AKTIENGESELLSCHAFT
Reel/Frame 064581/0893 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 20, 2023
From: LEWIS, TIMOTHY A.; GREULICH, HEIDI; WU, XIAOYUN; BURGIN, ALEX
To: THE BROAD INSTITUTE, INC.
Reel/Frame 063030/0809 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 20, 2023
From: MEYERSON, MATTHEW
To: DANA-FARBER CANCER INSTITUTE, INC.
Reel/Frame 063030/0952 →
Continuity (3)
Division 16635504
Provisional Application 62541627 · Aug 4, 2017
Related Publication 20220396554A1 · Dec 15, 2022
Cited By (2)
US 12,258,323 US 12,427,153