# US 8,785,457 B2 · Pyrimidine derivatives as mTOR inhibitors

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- Number: US 8,785,457 B2
- Document ID: US8785457B2
- Status: Granted
- Kind: B2
- Application number: 13/256,345
- Filed: 2010-03-12
- Published: 2012-03-15
- Granted: 2014-07-22
- Earliest claimed: 2009-03-13
- Assignees: Cellzome Limited
- Applicants: Rosemary Lynch; Andrew David Cansfield; Helen Sarah Niblock; Daniel Hardy; Jane Elizabeth Scanlon; Rita Adrego; Nigel Ramsden
- Inventors: Rosemary Lynch; Andrew David Cansfield; Helen Sarah Niblock; Daniel Hardy; Jane Elizabeth Scanlon; Rita Adrego; Nigel Ramsden
- Web page: https://patentgrep.com/patent/US8785457B2

## CPC

- C07D 413/04: directly linked by a ring-member-to-ring-member bond
- A61K 31/5377: not condensed and containing further heterocyclic rings, e.g. timolol
- A61P 3/00: Drugs for disorders of the metabolism (of the blood or the extracellular fluid A61P7/00)
- A61P 9/00: Drugs for disorders of the cardiovascular system
- A61P 25/28: for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
- 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 37/00: Drugs for immunological or allergic disorders
- A61P 37/06: Immunosuppressants, e.g. drugs for graft rejection
- A61P 37/08: Antiallergic agents (antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14)
- C07D 471/04: Ortho-condensed systems
- C07D 487/04: 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 invention relates to compounds of formula (I) wherein X, R1, R2, T, m, n, o have the meaning as cited in the description and the claims. The compounds of formula (I) are useful as inhibitors of mTOR for the treatment or prophylaxis of mTOR related diseases and disorders. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments.

## Claims

### Claim 1

A compound which is
(S)-1-cyclopropyl-3-(4-(4-(3-methylmorpholino)-6,7-dihydro-5H-pyrrolo[3,4-d]pyrimidin-2-yl)phenyl)urea, or a pharmaceutically acceptable salt thereof.

### Claim 2 (depends on 1)

A pharmaceutical composition comprising a compound or a pharmaceutically acceptable salt thereof of claim 1 together with a pharmaceutically acceptable carrier, optionally in combination with one or more other pharmaceutical compositions.

### Claim 3 (depends on 1)

A method of treating a mammalian patient in need thereof one or more conditions selected from the group consisting of diseases and disorders associated with mTOR, wherein the method comprises administering to said patient a therapeutically effective amount of a compound of claim 1 or a pharmaceutically acceptable salt thereof.

### Claim 4 (depends on 3)

The method of claim 3, wherein the disease or disorder is an immunological, inflammatory, autoimmune, or allergic disorder or disease or a transplant rejection or a Graft-versus host disease.

### Claim 5 (depends on 3)

The method of claim 3, wherein the disease is a proliferative disease.

### Claim 6 (depends on 3)

The method of claim 3, wherein the disease is a cardiovascular disease, a metabolic disease or a neurodegenerative disease.

### Claim 7 (depends on 3)

The method of claim 3, wherein the disease is an autophagy associated disease.

### Claim 8 (depends on 5)

The method of claim 5, wherein the proliferative disease is cancer.