Synthesis of N-(heteroaryl)-pyrrolo[3,2-d]pyrimidin-2-amines

Inventors: Alexander Smith (Apex, NC); Hannah S. White (Chapel Hill, NC); Francis Xavier Tavares (Durham, NC); Sergiy Krasutsky (Delmar, NY); Jian-Xie Chen (Albany, NY); Roberta L. Dorrow (Kalamazoo, MI); Hua Zhong (Boston, MA)

Assignee: G1 Therapeutics, Inc.

C07D487/20 C07D403/04 C07D487/14

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Quick Facts

Patent No.: US 11,629,150
App. No.: 17/121,392
Granted: Apr 18, 2023
Kind: B2

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Abstract

This invention is in the area of synthesizing pyrimidine-based compounds useful in the treatment of disorders involving abnormal cellular proliferation, including but not limited to tumors and cancers.

Claims (10)

1. A compound of Formula II:

wherein:

represents a carbocycle of 3 to 8 carbons connected in a spiro-fashion to the lactam ring;

R 1 is selected from alkyl, aryl, haloalkyl, and arylalkyl;

R 2 is selected from hydrogen, carbamate, aryl, alkyl, allyl, and arylalkyl; and

R 5 is selected from hydrogen, halogen, —N(alkyl)(alkoxy), —NCH 3 OMe, alkoxy, aryloxy, —OCH 2 aryl, —OC(O)alkyl, —OC(O)aryl, and —OC(O)arylalkyl.

2. The compound of claim 1 selected from:

3. The compound of claim 1 selected from:

4. The compound of claim 1 selected from:

5. The compound of claim 1 selected from:

Assignments (10)

ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 5, 2024

From: G1 THERAPEUTICS, INC.

To: PHARMACOSMOS A/S

Reel/Frame 069501/0882 →

ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 5, 2024

From: PHARMACOSMOS A/S

To: PHARMACOSMOS HOLDING A/S

Reel/Frame 069501/0891 →