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US 11,447,505 B1Granted
Pyrrolo[2,3-b]pyridine compounds and their use in the treatment of cancer
AssigneeCancer Research Technology Limited
InventorsAngelo Pugliese, Stuart Francis, Duncan McArthur, Mairi Sime, Justin Bower, Simone Belshaw
Life of this patent
Estimating the term…
Abstract
The present application relates to a compound of Formula I, or a salt, hydrate or solvate thereof, as defined herein. The present compounds are found to have pharmacological effects, particularly at MRCK. Further provided are pharmaceutical compositions comprising said compounds. The present invention also relates to the use of these compounds as therapeutic agents, in particular, for the treatment and/or prevention of proliferative diseases, such as cancer.
Claims15
A compound of Formula I, or a salt, hydrate or solvate thereof;
- wherein,
- R4 is a group of formula II,
- R3 is selected from 5-15 membered heteroaryl, where said 5-15 membered heteroaryl is optionally substituted by one or more Rb;
- each Rb is selected from hydrogen, hydroxyl, halogen, CN, C1-6 alkyl and O—C1-6 alkyl;
- wherein said C1-6 alkyl is optionally substituted with one or more groups selected from hydroxyl, halogen, ═O, NRcRd, C1-6 alkyl, O—C1-6 alkyl, and phenyl;
- each Rc is independently selected from hydrogen and C1-6 alkyl;
- each Rd is independently selected from hydrogen, CN, C1-6 haloalkyl, O—C1-6 haloalkyl, 3-7 membered heterocycloalkyl, 5-6 membered heteroaryl, C3-6cycloalkyl, C1-6 alkyl, O—C1-6 alkyl and phenyl, wherein said C1-6 alkyl, phenyl, 5-6 membered heteroaryl, 3-7 membered heterocycloalkyl and C3-6 cycloalkyl are optionally substituted with one or more groups selected from hydroxyl, halogen, CN, NH2, NH(C1-6alkyl), N(C1-6alkyl)2, C1-6 haloalkyl, C3-6 cycloalkyl, phenyl, 3-7 membered heterocycloalkyl, C3-10alkylheterocycloalkyl, C1-6 alkyl and O—C1-6 alkyl;
- or
- Rc and Rd, when attached to the same atom, together with the atom to which they are attached form a 3-7 membered heterocycloalkyl ring optionally substituted by one or more groups selected from hydroxyl, halogen, CN, NH2, NH(C1-6alkyl), N(C1-6 alkyl)2, C1-6 haloalkyl, O—C1-6 haloalkyl, C3-6 cycloalkyl, phenyl, 3-7 membered heterocycloalkyl, C1-6 alkyl and O—C1-6 alkyl;
- R5 is selected from hydrogen, halogen, hydroxyl, NH2, NH(C1-6 alkyl), N(C1-6 alkyl)2, C1-6 alkyl, O—C1-6 alkyl, C1-6 haloalkyl, O—C1-6 haloalkyl, C3-6 cycloalkyl, phenyl and CN;
- R9 and R10 are independently selected from hydroxyl, C1-6 alkyl, O—C1-6 alkyl, C1-6 haloalkyl, C1-6haloalkoxy, NH2, NH(C1-6alkyl), N(C1-6alkyl)2, NRcRd, NRcC(═O)Rd, C(O)NRcRd, phenyl, and 3-7 membered heterocycloalkyl, where said C1-6 alkyl, phenyl and 3-7 membered heterocycloalkyl are optionally substituted with one or more groups selected from halogen, hydroxyl, CN, NH2, NH(C1-6alkyl), N(C1-6alkyl)2, C1-6 alkyl, O—C1-6 alkyl, C1-6haloalkyl, C1-6haloalkoxy, C3-6 cycloalkyl and phenyl;
- or
- R9 and R10 together with the carbon atom to which they are attached form a 4-6 membered heterocycloalkyl ring comprising at least one heteroatom selected from O, N and S, where said heterocycloalkyl ring is optionally substituted with one or more Rm;
- Rm is selected from hydroxyl, halogen, CN, C1-6 alkyl, C3-6 cycloalkyl, C1-6 haloalkyl, and ORa;
- where Ra is defined above;
- and
- n is a number selected from 0 and 1.
14 more elements
Dependencies are inferred from the claim text.