# US 8,541,432 B2 · Heterobicyclic carboxamides as inhibitors for kinases

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- Number: US 8,541,432 B2
- Document ID: US8541432B2
- Status: Granted
- Kind: B2
- Application number: 13/613,053
- Filed: 2012-09-13
- Published: 2013-01-03
- Granted: 2013-09-24
- Earliest claimed: 2008-12-09
- Assignees: Novartis AG
- Applicants: Gerald David Artman, III; Jason Matthew Elliott; Nan Ji; Donglei Liu; Fupeng Ma; Nello Mainolfi; Erik Meredith; Karl Miranda; James J. Powers; Chang Rao
- Inventors: Gerald David Artman, III; Jason Matthew Elliott; Nan Ji; Donglei Liu; Fupeng Ma; Nello Mainolfi; Erik Meredith; Karl Miranda; James J. Powers; Chang Rao
- Web page: https://patentgrep.com/patent/US8541432B2

## CPC

- C07D 403/12: linked by a chain containing hetero atoms as chain links
- A61K 31/18: Sulfonamides (compounds containing a para-N-benzene-sulfonyl-N- group A61K31/63)
- A61K 31/404: Indoles, e.g. pindolol
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61P 3/10: for hyperglycaemia, e.g. antidiabetics
- 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 11/06: Antiasthmatics
- A61P 13/12: of the kidneys
- A61P 17/06: Antipsoriatics
- A61P 27/02: Ophthalmic agents
- 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 35/02: specific for leukemia
- A61P 37/00: Drugs for immunological or allergic disorders
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07D 403/14: containing three or more hetero rings
- C07D 413/14: containing three or more hetero rings
- C07D 471/04: Ortho-condensed systems
- C07D 487/04: Ortho-condensed systems
- C07D 487/08: Bridged 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 novel organic compounds of formula (I) and their use in the treatment of the animal or human body, to pharmaceutical compositions comprising a compound of formula I and to the use of a compound of formula I for the preparation of pharmaceutical compositions for use in the treatment of protein kinase dependent diseases, especially of proliferative diseases, such as in the treatment of tumour diseases and ocular neovascular diseases.

## Claims

### Claim 1

A compound, or a pharmaceutically acceptable salt thereof, according to the formula:

### Claim 2 (depends on 1)

A pharmaceutical composition comprising at least one compound of claim 1 and at least one pharmaceutically acceptable carrier.

### Claim 3 (depends on 1)

A method of treating a disorder or a disease in a subject mediated by VEGF-R, wherein the method comprises administering to the subject a therapeutically effective amount of the compound according to claim 1 and the disease or disorder is selected from age related macular degeneration, diabetic retinopathy, retinitis pigmentosa and retinopathy.