# US 11,439,646 B2 · Anti-proliferative agents for treating PAH

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- Number: US 11,439,646 B2
- Document ID: US11439646B2
- Status: Granted
- Kind: B2
- Application number: 17/089,154
- Filed: 2020-11-04
- Published: 2021-06-24
- Granted: 2022-09-13
- Earliest claimed: 2016-10-20
- Assignees: Pfizer Inc.
- Applicants: Pfizer Inc.
- Inventors: Steven Martin Evans
- Web page: https://patentgrep.com/patent/US11439646B2

## CPC

- A61K 31/519: ortho- or peri-condensed with heterocyclic rings
- A61K 31/506: not condensed and containing further heterocyclic rings
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61P 9/12: Antihypertensives
- A61P 11/00: Drugs for disorders of the respiratory system
- A61K 31/5575: having a cyclopentane, e.g. prostaglandin E2, prostaglandin F2-alpha
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

Pulmonary hypertension and related diseases, like pulmonary arterial hypertension, can be treated by administering an effective dose of a CDK inhibitor, including palbociclib, 6-acetyl-8-cyclopentyl-5-methyl-2-{[5-(piperazin-1-yl)pyridin-2yl]amino}pyrido[2,3-d]pyrimidin-7(8H)-one, or pharmaceutically acceptable salt thereof.

## Claims

### Claim 1

A method for treating pulmonary artery hypertension (PAH) in a human in need thereof, which method comprises administering to the human an effective amount of an inhibitor of CDK4 and CDK6 selected from the group consisting of:
6-acetyl-8-cyclopentyl-5-methyl-2-{[5-(piperazin-1-yl)pyridin-2yl]amino}pyrido[2,3-d[pyrimidin-7(8H)-one,
7-cyclopentyl-N, N-dimethyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxamide, or
2-pyrimidinamine, N-(5-((4-ethyl-1-piperazinyl)methyl)-2-pyridinyl)-5-fluoro-4-(4-fluoro-2-methyl-1-(1-methylethyl)-1H-benzimidazol-6-yl),
or pharmaceutically acceptable salts thereof.

### Claim 2 (depends on 1)

The method of claim 1, wherein the inhibitor of CDK4 and CDK6 is 7-cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxamide, or pharmaceutically acceptable salts thereof.

### Claim 3 (depends on 1)

The method of claim 1, wherein the inhibitor of CDK4 and CDK6 is 2-pyrimidinamine, N-(5-((4-ethyl-1-piperazinyl)methyl)-2-pyridinyl)-5-fluoro-4-(4-fluoro-2-methyl-1-(1-methylethyl)-1H-benzimidazol-6-yl), or pharmaceutically acceptable salts thereof.