IP Library › Granted Patent US 10,738,049
Granted Patent B2
US 10,738,049 · App. 16/340,874 · Granted Aug 11, 2020

N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodophenylamino)-6,8-dimethyl-2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-D]pyrimidin-1-YL]-phenyl}-cyclopropanecarboxamide dimethyl sulfoxide solvate as an MEK1/2 inhibitor

Inventors: Alexandre Vasilievich Ivachtchenko (Hallandale Beach, FL); Alexey Evgenievich Repik (Yaroslavl, RU); Vasily Gennadievich Ignatiev (Moscow, RU); Mikhail Airatovich Chafeev (Moscow, RU)
Assignee: R-PHARM JOINT STOCK COMPANY (R-PHARM, JSC)
C07D471/04A61P35/00A61K31/519C07B2200/13
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Quick Facts
Patent No.
US 10,738,049
App. No.
16/340,874
Granted
Aug 11, 2020
Kind
B2
Abstract

Novel MEK1, MEK2 and MEK1/2 inhibitors which have lower toxicity in long-term dosage, including the novel compound N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodophenylamino)-6,8-dimethyl-2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]-phenyl}-cyclopropanecarboxamide dimethyl sulfoxide solvate according to formula 1:

Claims (8)

1. A compound having a structure according to formula 1:

2. A pharmaceutically-acceptable composition comprising the compound of claim 1 as an active ingredient.

3. The pharmaceutically-acceptable composition of claim 2 , wherein the active ingredient exhibits inhibitor properties for one or both of MEK1 and MEK2.

4. The pharmaceutically-acceptable composition of claim 2 , wherein the active ingredient is present in a therapeutically effective amount.

5. The pharmaceutically-acceptable composition of claim 2 , further comprising one or more pharmaceutically acceptable excipients.

6. The pharmaceutically-acceptable composition of claim 2 , where the composition is in the form of tablets, capsules, or solutions for injection.

7. The pharmaceutically-acceptable composition of claim 6 , where the composition is placed in a pharmaceutically acceptable container.

8. A method of preparing a compound according to claim 1 , comprising treating a compound according to formula 2 or its salt, with cyclopropanecarboxylic acid or an activated derivative of cyclopropanecarboxylic acid

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 9, 2019
From: IVACHTCHENKO, ALEXANDRE VASILIEVICH; CHAFEEV, MIKHAIL AIRATOVICH; REPIK, ALEXEY EVGENIEVICH; IGNATIEV, VASILY GENNADIEVICH
To: R-PHARM JOINT STOCK COMPANY (R-PHARM, JSC); REPIK, ALEXEY EVGENIEVICH
Reel/Frame 050670/0652 →
Priority Claims (1)
RU 2016139641 · Oct 10, 2016 · national
Continuity (1)
Related Publication 20190233415A1 · Aug 1, 2019