# US 9,751,854 B2 · Heteroaryls and uses thereof

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- Number: US 9,751,854 B2
- Document ID: US9751854B2
- Status: Granted
- Kind: B2
- Application number: 15/347,334
- Filed: 2016-11-09
- Published: 2017-03-16
- Granted: 2017-09-05
- Earliest claimed: 2014-01-14
- Assignees: Millennium Pharmaceuticals, Inc.
- Applicants: Millennium Pharmaceuticals, Inc.
- Inventors: Indu T. Bharathan; Chris Blackburn; Jeffrey P. Ciavarri; Jouhara Chouitar; Courtney A. Cullis; Natalie D'Amore; Paul E. Fleming; Kenneth M. Gigstad; Krista E. Gipson; Mario Girard; Yongbo Hu; Janice Lee; Gang Li; Mansoureh Rezaei; Michael D. Sintchak; Francois Soucy; Stephen G. Stroud; Tricia J. Vos; Tzu-Tshin Wong; He Xu; Tianlin Xu; Yingchun Ye
- Web page: https://patentgrep.com/patent/US9751854B2

## CPC

- C07D 513/04: Ortho-condensed systems
- A61K 31/437: the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
- A61K 31/444: containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
- A61K 31/497: containing further heterocyclic rings
- A61K 31/506: not condensed and containing further heterocyclic rings
- A61K 31/549: having two or more nitrogen atoms in the same ring, e.g. hydrochlorothiazide
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61P 7/02: Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
- A61P 9/00: Drugs for disorders of the cardiovascular system
- A61P 9/04: Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
- A61P 9/10: for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
- A61P 9/12: Antihypertensives
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 35/00: Antineoplastic agents
- A61P 37/02: Immunomodulators
- A61P 37/08: Antiallergic agents (antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14)
- C07D 401/04: directly linked by a ring-member-to-ring-member bond
- C07D 401/14: containing three or more hetero rings
- C07D 417/14: containing three or more hetero rings
- C07D 471/04: Ortho-condensed systems
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- 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

The present invention provides a compound of formula I: and pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, R4, R5, L1, L2, m, and n, are as described in the specification. Such compounds are inhibitors of VPS34 and thus useful for treating proliferative, inflammatory, or cardiovascular disorders.

## Claims

### Claim 1

A compound selected from the group consisting of:
or a pharmaceutically acceptable salt thereof.

### Claim 2 (depends on 1)

The compound of claim 1, which is
or a pharmaceutically acceptable salt thereof.

### Claim 3 (depends on 1)

The compound of claim 1, which is
or a pharmaceutically acceptable salt thereof.

### Claim 4 (depends on 1)

The compound of claim 1, which is
or a pharmaceutically acceptable salt thereof.

### Claim 5 (depends on 1)

A pharmaceutical composition comprising the compound of claim 1 or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.

### Claim 6 (depends on 5)

The pharmaceutical composition of claim 5, wherein the compound is
or a pharmaceutically acceptable salt thereof.

### Claim 7 (depends on 5)

The pharmaceutical composition of claim 5, wherein the compound is
or a pharmaceutically acceptable salt thereof.

### Claim 8 (depends on 5)

The pharmaceutical composition of claim 5, wherein the compound is
or a pharmaceutically acceptable salt thereof.