1,2,4-triazine-4-amine derivatives

Patent metadata

Field	Value
Publication number	US-10112923-B2
Application number	US-201615344048-A
Country	US
Kind code	B2
Filing date	Nov 4, 2016
Priority date	Feb 5, 2010
Publication date	Oct 30, 2018
Grant date	Oct 30, 2018

Abstract

According to the invention there is provided a compound of formula A1 which may be useful in the treatment of a condition or disorder ameliorated by the inhibition of the A 1 -A 2b or, particularly, the A 2a receptor wherein the compound of formula A1 has the structure, wherein, A represents Cy 1 or Het A ; Cy 1 represents a 5- to 14-membered aromatic, fully saturated or partially unsaturated carbocylic ring system comprising one, two or three rings, which Cy 1 group is optionally substituted by one or more R 4a substituents; Het A represents a 5- to 14-membered heterocyclic group that may be aromatic, fully saturated or partially unsaturated, and which contains one or more heteroatoms selected from O, S and N, which heterocyclic group may comprise one, two or three rings and which HetA group is optionally substituted by one or more R4b substituents; B represents a Cy 2 or Het B ; Cy 2 represents a 3- to 10-membered aromatic, fully saturated or partially unsaturated carbocyclic ring system comprising one or two rings, which Cy 2 group is optionally substituted by one or more R 4c substituents; Het B represents a 3- to 10-membered heterocyclic group that may be aromatic, fully saturated or partially unsaturated, and which contains one or more heteroatoms selected from O, S and N, which heterocyclic group may comprise one or two rings and which Het B group is optionally substituted by one or more R 4d substituents.

First claim

The invention claimed is:

1. A method of treatment of cancer, comprising administering an effective amount of 6-(2-chloro-6-methylpyridin-4-yl)-5-(4-fluorophenyl)-1,2,4-triazin-3-amine, or a pharmaceutically acceptable salt or solvate, to a patient in need of such treatment, wherein the cancer is selected from the group consisting of prostate cancer, rectal cancer, renal cancer, ovarian cancer, endometrial cancer, thyroid cancer, pancreatic cancer, breast cancer, colon cancer, bladder cancer, brain cancer, glia cancer, melanoma cancer, pineal gland cancer, and lung cancer.

2. The method as claimed in claim 1 , wherein the cancer is selected from the group consisting of rectal cancer, pancreatic cancer, colon cancer, brain cancer, glia cancer, and lung cancer.

3. A compound, wherein the compound is 6-(2-chloro-6-methylpyridin-4-yl)-5-(4-fluorophenyl)-1,2,4-triazin-3-amine, or a pharmaceutically acceptable salt or solvate.

Assignees

• Heptares Therapeutics Ltd

Inventors

• Congreve Miles Stuart
• Andrews Stephen Philippe
• Mason Jonathan Stephen
• Richardson Christine Mary
• Brown Giles Albert

Classifications

• A61P9/00

  Drugs for disorders of the cardiovascular system · CPC title

• A61P3/10

  for hyperglycaemia, e.g. antidiabetics · CPC title

• A61P43/00

  Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title

• A61P35/00

  Antineoplastic agents · CPC title

• A61P7/10

  Antioedematous agents; Diuretics · CPC title