US 9,309,252 B2Granted

Pyrrolopyrimidine compounds as inhibitors of CDK4/6

AssigneeNovartis AG

InventorsChristopher Thomas Brain, Young Shin Cho, John William Giraldes, Bharat Lagu, Julian Roy Levell, Michael Joseph Luzzio, Lawrence Blas Perez, Yaping Wang, Fan Yang

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Abstract

The invention is directed to novel pyrrolopyrimidine compounds of formula (1) wherein R1, R2y, R4, R8-R11, A and L are defined herein and to salts, including pharmaceutically acceptable salts thereof. The compounds of the present invention are CDK4/6 inhibitors and could be useful in the treatment of diseases and disorders mediated by CDK4/6, such as cancer, including mantle cell lymphoma, liposarcoma, non small cell lung cancer, melanoma, squamous cell esophageal cancer and breast cancer. The invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting CDK4/6 activity and to the treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.

Claims18

Dependent claims

A method for the treatment of a carcinoma with genetic aberrations that activate CDK 4/6 kinase activity in a patient in need of treatment thereof comprising administration of an effective amount of a compound selected from the group consisting of:

7-cyclopentyl-N,N-dimethyl-2-(5-((1R,6S)-9-methyl-4-oxo-3,9-diazabicyclo[4.2.1]nonan-3-yl)pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxamide;
7-Cyclopentyl-2-[5-(3,8-diaza-bicyclo[3.2.1]octane-3-carbonyl)-pyridin-2-ylamino]-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide;
7-Cyclopentyl-2-[5-((1R,6S)-4-oxo-3,9-diaza-bicyclo[4.2.1]non-3-yl)-pyridin-2-ylamino]-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide;
7-Cyclopentyl-2-[5-((1R,6S)-4-oxo-3,9-diaza-bicyclo[4.2.1]non-3-yl)-pyridin-2-ylamino]-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid methylamide;
and
7-Cyclopentyl-2-[5-((1R,6S)-4-oxo-3,9-diaza-bicyclo[4.2.1]non-3-yl)-pyridin-2-ylamino]-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid methylamide;
or a pharmaceutically acceptable salt thereof.

4 more elements

Dependencies are inferred from the claim text.

Facts

Application: 14/568,410Filed 12 Dec 2014 · continuation
Priority: 19 Feb 2010
Published: US 2015/0099737 A19 Apr 2015
Granted: 12 Apr 2016
Term ends: Not estimatedThe source records don’t support an estimate.

Classification15 codes

C07D 487/04
In which the condensed system contains two hetero rings: ortho-condensed systems
A61P 35/00
Antineoplastic agents
A61P 35/02
Antineoplastic agents: specific for leukemia
C07B 59/002
Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se: heterocyclic compounds

Family

Application61/306,248Us provisional application · filed 19 Feb 2010
Application61/429,372Us provisional application · filed 3 Jan 2011
Application61/429,997Us provisional application · filed 5 Jan 2011
PCT/EP2011/052353Parent of this continuation · filed 17 Feb 2011
US 2015/0099737 A1Pre-grant publication · published 9 Apr 2015
Application13/579,359Parent of this continuation
US 8,957,074 B2Parent of this continuation
US 2013/0150342 A1Published application
US 9,309,252 B2This patent

From the US filing history. Foreign family members aren’t listed.