http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-116507-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_a73cee5001ad08339ae751c10d9abf71 |
| classificationCPCAdditional | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K45-06 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D487-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D487-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D519-00 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-519 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D487-04 |
| filingDate | 2019-09-25-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_2b132d36eb2519e6fc743d9f1059fbae http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_dbacfbf86d3828a5cc6251bf3d919d08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_1891e0bd6a763df157313299f489621f http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_ecbe9664a4ed9d8adabf23b5fa03fc61 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_e5aa9adb79b91cc60a0082ed1f17b426 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_fe9765c13d8bc4bd1d1ad1f5e47afe0f http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_eaa19a398604efb5f2d88b49fb9e0bc7 |
| publicationDate | 2021-05-12-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-116507-A1 |
| titleOfInvention | PYRAZOLOPYRIMIDINE COMPOUNDS AND USES OF THEM |
| abstract | Compounds of formula (1), methods for using the compounds to inhibit ALK2 activity and / or FGFR activity, and pharmaceutical compositions comprising said compounds are described. The compounds are useful for the treatment, prevention or amelioration of diseases or disorders associated with ALK2 activity and / or FGFR activity, such as cancer. Claim 1: A compound of formula (1), or a pharmaceutically acceptable salt thereof, characterized in that: R¹ is selected from Cy¹, C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₁₋₆ haloalkyl, halo, CN, NO₂, ORᵃ, SRᵃ, C (O) Rᵇ, C (O) NRᶜRᵈ, C (O) ORᵃ, OC (O) Rᵇ, OC (O) NRᶜRᵈ, NRᶜRᵈ, NRᶜC (O) Rᵇ, NRᶜC (O) ORᵃ, NRᶜC (O) NRᶜRᵈ, C (= NRᵉ) Rᵇ, C (= NORᵃ) Rᵇ, C (= NRᵉ) NRᶜRᵈ, NRᶜC (= NRᵉ) NRᶜRᵈ, NRᶜS (O) Rᵇ, NRᶜS (O) ₂Rᵇ, NRᶜS ( O) ₂NRᶜRᵈ, S (O) Rᵇ, S (O) NRᶜRᵈ, S (O) ₂Rᵇ and S (O) ₂NRᶜRᵈ; wherein said C₁₋₆ alkyl, C₂₋₆ alkenyl and C₂₋₆ alkynyl are substituted with 1, 2, 3 or 4 substituents independently selected from R¹⁰; Cy¹ is selected from C₄₋₈ cycloalkyl, 4-12 membered heterocycloalkyl, C₆₋₁₀ aryl, and 5-10 membered heteroaryl; wherein 4-12 membered heterocycloalkyl and 5-10 membered heteroaryl have at least one ring-forming carbon atom and 1, 2, 3, or 4 ring-forming heteroatoms independently selected from N, O, and S; where N and S are optionally oxidized; wherein a ring-forming carbon atom of 5-10 membered heteroaryl and 4-12 membered heterocycloalkyl are optionally substituted with oxo to form a carbonyl group; and wherein C₄₋₈ cycloalkyl, 4-12 membered heterocycloalkyl, C₆₋₁₀ aryl and 5-10 membered heteroaryl are optionally substituted with 1, 2, 3 or 4 substituents independently selected from R¹⁰; Cy is 4-12 membered heterocycloalkyl; wherein the 4-12 membered heterocycloalkyl has at least one ring-forming carbon atom and 1, 2, 3, or 4 ring-forming heteroatoms independently selected from N, O, and S; where N and S are optionally oxidized; wherein a 4-12 membered heterocycloalkyl ring-forming carbon atom is optionally substituted by oxo to form a carbonyl group; wherein when the 4-12 membered heterocycloalkyl of Cy has a fused aromatic ring, the 4-12 membered heterocycloalkyl is directly attached to the pyrazolopyrimidine core structure through a saturated or partially saturated ring-forming ring atom; and wherein the 4-12 membered heterocycloalkyl is optionally substituted with 1, 2, 3, 4, or 5 substituents independently selected from R²⁰; R² is selected from H, D, C₁₋₄ alkyl, C₁₋₄ haloalkyl, C₁₋₄ alkoxy, and C₁₋₄ haloalkoxy; each R¹⁰ is independently selected from C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₁₋₆ haloalkyl, C₃₋₁₀ cycloalkyl, 4-10 membered heterocycloalkyl, C₆₋₁₀ aryl, 5-10 membered heteroaryl, C₃₋₁₀cycloalkyl-C₁₋₃ alkylene, 4-10 membered heterocycloalkyl-C₁₋₃ alkylene, C₆₋₁₀ aryl-C₁₋₃ alkylene, 5-10 membered heteroaryl-C₁₋₃ alkylene, halo, D, CN, NO₂, ORᵃ¹, SRᵃ¹, C (O) Rᵇ¹, C (O) NRᶜ¹Rᵈ¹, C (O) ORᵃ¹, OC (O) Rᵇ¹, OC (O) NRᶜ¹Rᵈ¹, NRᶜ¹Rᵈ¹, NRᶜ¹C (O) Rᵇ¹, NRᶜ¹C (O) ORᵃ¹, NRᶜ¹C (O) NRᶜ¹Rᵈ¹, C (= NRᵉ¹) Rᵇ¹, C (= NORᵃ¹) Rᵇ¹, C (= NRᵉ¹) NRᶜ¹Rᵈ¹, NRᶜ¹C (= NRᵉ¹) NRᶜ¹Rᵈ¹, NRᶜ¹S (O) Rᵇ¹, NRᶜ¹S (O) ₂Rᵇ¹, NRᶜ¹S (O) ₂NRᶜ¹Rᵈ¹, S (O) Rᵇ¹, S (O) NRᶜ¹Rᵈ¹, S (O) ₂Rᵇ¹ and S (O) ₂NRᶜ¹Rᵈ¹; wherein said C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₃₋₁₀ cycloalkyl, 4-10 membered heterocycloalkyl, C₆₋₁₀ aryl, 5-10 membered heteroaryl, C₃₋₁₀ cycloalkyl-C₁₋ alkylene *, 4-10 membered heterocycloalkyl-C₁₋₃ alkylene, C₆₋₁₀ aryl-C₁₋₃ alkylene, and 5-10 membered heteroaryl-C₁₋₃ alkylene are optionally substituted with 1, 2, 3, or 4 substituents independently selected from R¹¹; or two R¹⁰ substituents together with the carbon atom to which they are attached, form a 4-7 membered spiro heterocycloalkyl ring or a C₃₋₆ spiro cycloalkyl ring; wherein each spiro-membered 4-7 heterocycloalkyl ring has at least one ring-forming carbon atom and 1, 2, or 3 ring-forming heteroatoms independently selected from N, O, and S; wherein one ring-forming carbon atom of each spiro 4-7 membered heterocycloalkyl ring is optionally substituted by oxo to form a carbonyl group; and wherein the spiro 4-7 membered heterocycloalkyl ring and C₃₋₆ spiro cycloalkyl ring are optionally substituted with 1, 2, 3, or 4 substituents independently selected from R¹¹; each R¹¹ is independently selected from C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₁₋₆ haloalkyl, C₃₋₁₀ cycloalkyl, 4-10 membered heterocycloalkyl, C₆₋₁₀ aryl, 5- 10 membered heteroaryl, C₃₋₁₀cycloalkyl-C₁₋₃ alkylene, 4-10 membered heterocycloalkyl-C₁₋₃ alkylene, C₆₋₁₀ aryl-C₁₋₃ alkylene, 5-10 membered heteroaryl-C₁₋₃ alkylene, halo, D, CN, ORᵃ³, SRᵃ³, C (O) Rᵇ³, C (O) NRᶜ³Rᵈ³, C (O) ORᵃ³, NRᶜ³Rᵈ³, NRᶜ³C (O) Rᵇ³, NRᶜ³C (O) ORᵃ³, NRᶜ³S (O) Rᵇ³, NRᶜ³S (O) ₂RᵇS³, NRᶜ³S (O) ₂RᵇS³ O) ₂NRᶜ³Rᵈ³, S (O) Rᵇ³, S (O) NRᶜ³Rᵈ³, S (O) ₂Rᵇ³ and S (O) ₂NRᶜ³Rᵈ³; wherein said C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₃₋₁₀ cycloalkyl, 4-10 membered heterocycloalkyl, C₆₋₁₀ aryl, 5-10 membered heteroaryl, C₃₋₁₀ cycloalkyl-C₁₋ alkylene *, 4-10 membered heterocycloalkyl-C₁₋₃ alkylene, C₆₋₁₀ aryl-C₁₋₃ alkylene, and 5-10 membered heteroaryl-C₁₋₃ alkylene are optionally substituted with 1, 2, 3, or 4 substituents independently selected from R¹²; each R¹² is independently selected from C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₁₋₆ haloalkyl, C₃₋₆ cycloalkyl, C₆₋₁₀ aryl, 5-10 membered heteroaryl, 4-7 membered heterocycloalkyl, C₃₋₆cycloalkyl-C₁₋₃ alkylene, 4-7 membered heterocycloalkyl-C₁₋₃ alkylene, C₆₋₁₀ aryl-C₁₋₃ alkylene, 5-10 membered heteroaryl-C₁₋₃ alkylene, halo, D, CN, ORᵃ⁵, SRᵃ⁵, C (O) Rᵇ⁵, C (O) NRᶜ⁵Rᵈ⁵, C (O) ORᵃ⁵, NRᶜ⁵Rᵈ⁵, NRᶜ⁵C (O) Rᵇ⁵, NRᶜ⁵C (O) ORᵃ⁵, NRᶜ⁵S (O) Rᵇ⁵, NRᶜ⁵S (O) ₂Rᵇ⁵, NRᶜ⁵S ( O) ₂NRᶜ⁵Rᵈ⁵, S (O) Rᵇ⁵, S (O) NRᶜ⁵Rᵈ⁵, S (O) ₂Rᵇ⁵ and S (O) ₂NRᶜ⁵Rᵈ⁵; wherein said C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₃₋₆ cycloalkyl, C₆₋₁₀ aryl, 5-10 membered heteroaryl, 4-7 membered heterocycloalkyl, C₃₋₆ cycloalkyl-C₁₋ alkylene *, 4-7 membered heterocycloalkyl-C₁₋₃ alkylene, C₆₋₁₀ aryl-C₁₋₃ alkylene, and 5-10 membered heteroaryl-C₁₋₃ alkylene are optionally substituted with 1, 2, 3, or 4 substituents independently selected from Rᵍ; each R²⁰ is independently selected from C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₁₋₆ haloalkyl, C₃₋₁₀ cycloalkyl, 4-10 membered heterocycloalkyl, C₆₋₁₀ aryl, 5-10 membered heteroaryl, C₃₋₁₀cycloalkyl-C₁₋₃ alkylene, 4-10 membered heterocycloalkyl-C₁₋₃ alkylene, C₆₋₁₀ aryl-C₁₋₃ alkylene, 5-10 membered heteroaryl-C₁₋₃ alkylene, halo, D, CN, NO₂, ORᵃ², SRᵃ², C (O) Rᵇ², C (O) NRᶜ²Rᵈ², C (O) ORᵃ², OC (O) Rᵇ², OC (O) NRᶜ²Rᵈ², NRᶜ²Rᵈ², NRᶜ²C (O) Rᵇ², NRᶜ²C (O) ORᵃ², NRᶜ²C (O) NRᶜ²Rᵈ², C (= NRᵉ²) Rᵇ², C (= NORᵃ²) Rᵇ², C (= NRᵉ²) NRᶜ²Rᵈ², NRᶜ²C (= NRᵉ²) NRᶜ²Rᵈ², NRᶜ²S (O) Rᵇ², NRᶜ²RS (O) ² ₂NRᶜ²Rᵈ², S (O) Rᵇ², S (O) NRᶜ²Rᵈ², S (O) ₂Rᵇ² and S (O) ₂NRᶜ²Rᵈ²; wherein said C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₃₋₁₀ cycloalkyl, 4-10 membered heterocycloalkyl, C₆₋₁₀ aryl, 5-10 membered heteroaryl, C₃₋₁₀ cycloalkyl-C₁₋ alkylene *, 4-10 membered heterocycloalkyl-C₁₋₃ alkylene, C₆₋₁₀ aryl-C₁₋₃ alkylene, and 5-10 membered heteroaryl-C₁₋₃ alkylene are optionally substituted with 1, 2, 3, or 4 substituents independently selected from R²¹; each R²¹ is independently selected from C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₁₋₆ haloalkyl, C₃₋₁₀ cycloalkyl, 4-10 membered heterocycloalkyl, C₆₋₁₀ aryl, 5-10 membered heteroaryl, C₃₋₁₀cycloalkyl-C₁₋₃ alkylene, 4-10 membered heterocycloalkyl-C₁₋₃ alkylene, C₆₋₁₀ aryl-C₁₋₃ alkylene, 5-10 membered heteroaryl-C₁₋₃ alkylene, halo, D, CN, ORᵃ⁴, SRᵃ⁴, C (O) Rᵇ⁴, C (O) NRᶜ⁴Rᵈ⁴, C (O) ORᵃ⁴, NRᶜ⁴Rᵈ⁴, NRᶜ⁴C (O) Rᵇ⁴, NRᶜ⁴C (O) ORᵃ⁴, NRᶜ⁴S (O) Rᵇ⁴, NRᶜ⁴S (O) ₂Rᵇ⁴, NRᶜ⁴S ( O) ₂NRᶜ⁴Rᵈ⁴, S (O) Rᵇ⁴, S (O) NRᶜ⁴Rᵈ⁴, S (O) ₂Rᵇ⁴ and S (O) ₂NRᶜ⁴Rᵈ⁴; wherein said C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₃₋₁₀ cycloalkyl, 4-10 membered heterocycloalkyl, C₆₋₁₀ aryl, 5-10 membered heteroaryl, C₃₋₁₀ cycloalkyl-C₁₋ alkylene *, 4-10 membered heterocycloalkyl-C₁₋₃ alkylene, C₆₋₁₀ aryl-C₁₋₃ alkylene, and 5-10 membered heteroaryl-C₁₋₃ alkylene are optionally substituted with 1, 2, 3, or 4 substituents independently selected from R²²; each R²² is independently selected from C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₁₋₆ haloalkyl, C₃₋₆ cycloalkyl, phenyl, 5-6 membered heteroaryl, 4-7 membered heterocycloalkyl, C₃₋ cycloalkyl ₆-C₁₋₃ alkylene, 4-7 membered heterocycloalkyl-C₁₋₃ alkylene, phenyl-C₁₋₃ alkylene, 5-6 membered heteroaryl-C₁₋₃ alkylene, halo, D, CN, ORᵃ⁶, SRᵃ⁶, C ( O) Rᵇ⁶, C (O) NRᶜ⁶Rᵈ⁶, C (O) ORᵃ⁶, NRᶜ⁶Rᵈ⁶, NRᶜ⁶C (O) Rᵇ⁶, NRᶜ⁶C (O) ORᵃ⁶, NRᶜ⁶S (O) Rᵇ⁶, NRᶜ⁶S (O) ₂Rᵇ⁶, NRᶜ⁶S (O) ₂NRᶜ⁶Rᵈ⁶, S ( O) Rᵇ⁶, S (O) NRᶜ⁶Rᵈ⁶, S (O) ₂Rᵇ⁶ and S (O) ₂NRᶜ⁶Rᵈ⁶; wherein said C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₃₋₆ cycloalkyl, phenyl, 5-6 membered heteroaryl, 4-7 membered heterocycloalkyl, C₃₋₆-C₁₋₃ alkylene cycloalkyl, heterocycloalkyl 4-7-membered C₁₋₃ alkylene, phenyl-C₁₋₃ alkylene and 5-6 membered heteroaryl-C₁₋₃ alkylene are optionally substituted with 1, 2, 3, or 4 substituents independently selected from Rᵍ; each Rᵃ, Rᶜ, and Rᵈ is independently selected from H, C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₁₋₆ haloalkyl, C₃₋₁₀ cycloalkyl, 4-10 membered heterocycloalkyl, C₆₋₁₀ aryl, heteroaryl 5-10 membered, C₃₋₁₀-C₁₋₃ cycloalkyl, 4-10 membered heterocycloalkyl-C₁₋₃ alkylene, C₆₋₁₀ aryl-C₆₋₁₀ alkylene and 5-10 membered heteroaryl-C₁₋₃ alkylene; wherein said C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₃₋₁₀ cycloalkyl, 4-10 membered heterocycloalkyl, C₆₋₁₀ aryl, 5-10 membered heteroaryl, C₃₋₁₀ cycloalkyl-C₁₋ alkylene *, 4-10 membered heterocycloalkyl-C₁₋₃ alkylene, C₆₋₁₀ aryl-C₁₋₃ alkylene, and 5-10 membered heteroaryl-C₁₋₃ alkylene are optionally substituted with 1, 2, 3, or 4 substituents independently selected from R¹⁰; or any Rᶜ and Rᵈ attached to the same N atom, together with the N atom to which they are attached, form a 4-10 membered heterocycloalkyl group optionally substituted with 1, 2, 3 or 4 substituents independently selected from R¹⁰; each Rᵇ is independently selected from C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₁₋₆ haloalkyl, C₃₋₁₀ cycloalkyl, 4-10 membered heterocycloalkyl, C₆₋₁₀ aryl, 5-10 membered heteroaryl, C₃₋₁₀cycloalkyl-C₁₋₃ alkylene, 4-10 membered heterocycloalkyl-C₁₋₃ alkylene, C₆₋₁₀ aryl-C₁₋₃ alkylene and 5-10 membered heteroaryl-C₁₋₃ alkylene; wherein said C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₃₋₁₀ cycloalkyl, 4-10 membered heterocycloalkyl, C₆₋₁₀ aryl, 5-10 membered heteroaryl, C₃₋₁₀ cycloalkyl-C₁₋ alkylene *, 4-10 membered heterocycloalkyl-C₁₋₃ alkylene, C₆₋₁₀ aryl-C₁₋₃ alkylene, and 5-10 membered heteroaryl-C₁₋₃ alkylene are optionally substituted with 1, 2, 3, or 4 substituents independently selected from R¹⁰; each Rᵉ is independently selected from H, CN, C₁₋₆ alkyl, C₁₋₆ haloalkyl, C₁₋₆ alkylthio, C₁₋₆ alkylsulfonyl, C₁₋₆ alkylcarbonyl, carbamyl, C₁₋₆ alkylcarbamyl, di (C₁₋₆ alkyl) carbamyl , aminosulfonyl, C₁₋₆ alkylaminosulfonyl and di (C₁₋₆ alkyl) aminosulfonyl; each Rᵃ¹, Rᶜ¹, and Rᵈ¹ is independently selected from H, C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₁₋₆ haloalkyl, C₃₋₁₀ cycloalkyl, 4-10 membered heterocycloalkyl, C₆₋₁₀ aryl, heteroaryl 5-10 membered, C₃₋₁₀ cycloalkyl-C₁₋₃ alkylene, 4-10 membered heterocycloalkyl-C₁₋₃ alkylene, C₆₋₁₀ aryl-C₁₋₃ alkylene and 5-10 membered heteroaryl-C₁₋₃ alkylene; wherein said C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₃₋₁₀ cycloalkyl, 4-10 membered heterocycloalkyl, C₆₋₁₀ aryl, 5-10 membered heteroaryl, C₃₋₁₀ cycloalkyl-C₁₋ alkylene *, 4-10 membered heterocycloalkyl-C₁₋₃ alkylene, C₆₋₁₀ aryl-C₁₋₃ alkylene, and 5-10 membered heteroaryl-C₁₋₃ alkylene are optionally substituted with 1, 2, 3, or 4 substituents independently selected from R¹¹; or any Rᶜ¹ and Rᵈ¹ attached to the same N atom, together with the N atom to which they are attached, form a 4-10 membered heterocycloalkyl group optionally substituted with 1, 2, 3 or 4 substituents independently selected from R¹¹; each Rᵇ¹ is independently selected from C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₁₋₆ haloalkyl, C₃₋₁₀ cycloalkyl, 4-10 membered heterocycloalkyl, C₆₋₁₀ aryl, 5- 10 membered heteroaryl, C₃₋₁₀cycloalkyl-C₁₋₃ alkylene, 4-10 membered heterocycloalkyl-C₁₋₃ alkylene, C₆₋₁₀ aryl-C₁₋₃ alkylene and 5-10 membered heteroaryl-C₁₋₃ alkylene; wherein said C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₃₋₁₀ cycloalkyl, 4-10 membered heterocycloalkyl, C₆₋₁₀ aryl, 5-10 membered heteroaryl, C₃₋₁₀ cycloalkyl-C₁₋ alkylene *, 4-10 membered heterocycloalkyl-C₁₋₃ alkylene, C₆₋₁₀ aryl-C₁₋₃ alkylene, and 5-10 membered heteroaryl-C₁₋₃ alkylene are optionally substituted with 1, 2, 3, or 4 substituents independently selected from R¹¹; each Rᵉ¹ is independently selected from H, CN, C₁₋₆ alkyl, C₁₋₆ haloalkyl, C₁₋₆ alkylthio, C₁₋₆ alkylsulfonyl, C₁₋₆ alkylcarbonyl, C₁₋₆ alkylaminosulfonyl, carbamyl, C₁₋₆ alkylcarbamyl, di (alkyl C₁₋₆) carbamyl, aminosulfonyl, C₁₋₆ alkylaminosulfonyl and di (C₁₋₆ alkyl) aminosulfonyl; each Rᵃ², Rᶜ² and Rᵈ² is independently selected from H, C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₁₋₆ haloalkyl, C₃₋₁₀ cycloalkyl, 4-10 membered heterocycloalkyl, C₆₋₁₀ aryl, heteroaryl 5-10 membered, C₃₋₁₀ cycloalkyl-C₁₋₃ alkylene, 4-10 membered heterocycloalkyl-C₁₋₃ alkylene, C₆₋₁₀ aryl-C₁₋₃ alkylene and 5-10 membered heteroaryl-C₁₋₃ alkylene; wherein said C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₃₋₁₀ cycloalkyl, 4-10 membered heterocycloalkyl, C₆₋₁₀ aryl, 5-10 membered heteroaryl, C₃₋₁₀ cycloalkyl-C₁₋ alkylene *, 4-10 membered heterocycloalkyl-C₁₋₃ alkylene, C₆₋₁₀ aryl-C₁₋₃ alkylene, and 5-10 membered heteroaryl-C₁₋₃ alkylene are optionally substituted with 1, 2, 3, or 4 substituents independently selected from R²¹; or any Rᶜ² and Rᵈ² attached to the same N atom, together with the N atom to which they are attached, form a 4-10 membered heterocycloalkyl group optionally substituted with 1, 2, 3 or 4 substituents independently selected from R²¹; each Rᵇ² is independently selected from C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₁₋₆ haloalkyl, C₃₋₁₀ cycloalkyl, 4-10 membered heterocycloalkyl, C₆₋₁₀ aryl, 5-10 membered heteroaryl, C₃₋₁₀cycloalkyl-C₁₋₃ alkylene, 4-10 membered heterocycloalkyl-C₁₋₃ alkylene, C₆₋₁₀ aryl-C₁₋₃ alkylene and 5-10 membered heteroaryl-C₁₋₃ alkylene; wherein said C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₃₋₁₀ cycloalkyl, 4-10 membered heterocycloalkyl, C₆₋₁₀ aryl, 5-10 membered heteroaryl, C₃₋₁₀ cycloalkyl-C₁₋ alkylene *, 4-10 membered heterocycloalkyl-C₁₋₃ alkylene, C₆₋₁₀ aryl-C₁₋₃ alkylene, and 5-10 membered heteroaryl-C₁₋₃ alkylene are optionally substituted with 1, 2, 3, or 4 substituents independently selected from R²¹; each Rᵉ² is independently selected from H, CN, C₁₋₆ alkyl, C₁₋₆ haloalkyl, C₁₋₆ alkylthio, C₁₋₆ alkylsulfonyl, C₁₋₆ alkylcarbonyl, C₁₋₆ alkylaminosulfonyl, carbamyl, C₁₋₆ alkylcarbamyl, di (alkyl C₁₋₆) carbamyl, aminosulfonyl, C₁₋₆ alkylaminosulfonyl and di (C₁₋₆ alkyl) aminosulfonyl; each Rᵃ³, Rᶜ³ and Rᵈ³ is independently selected from H, C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₁₋₆ haloalkyl, C₃₋₆ cycloalkyl, phenyl, 5-6 membered heteroaryl, 4-4 heterocycloalkyl 7-membered, C₃₋₆ cycloalkyl-C₁₋₃ alkylene, 4-7 membered heterocycloalkyl-C₁₋₃ alkylene, phenyl-C₁₋₃ alkylene and 5-6 membered heteroaryl-C₁₋₃ alkylene; wherein said C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₃₋₆ cycloalkyl, phenyl, 5-6 membered heteroaryl, 4-7 membered heterocycloalkyl, C₃₋₆-C₁₋₃ alkylene cycloalkyl, heterocycloalkyl 4-7-membered C alqu alkylene, phenyl-C₁₋₃ alkylene, and 5-6 membered heteroaryl-C₁₋₃ alkylene are each optionally substituted with 1, 2, 3, or 4 substituents independently selected from R¹²; or any Rᶜ³ and Rᵈ³ attached to the same N atom, together with the N atom to which they are attached, form a 4-, 5-, 6- or 7-membered heterocycloalkyl group optionally substituted with 1, 2 or 3 substituents independently selected from R¹²; each Rᵇ³ is independently selected from C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₁₋₆ haloalkyl, C₃₋₆ cycloalkyl, phenyl, 5-6 membered heteroaryl, 4-7 membered heterocycloalkyl, C₃₋ cycloalkyl ₆-C₁₋₃ alkylene, 4-7 membered heterocycloalkyl-C₁₋₃ alkylene, phenyl-C₁₋₃ alkylene and 5-6 membered heteroaryl-C₁₋₃ alkylene; wherein said C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₃₋₆ cycloalkyl, phenyl, 5-6 membered heteroaryl, 4-7 membered heterocycloalkyl, C₃₋₆-C₁₋₃ alkylene cycloalkyl, heterocycloalkyl 4-7-membered C alqu alkylene, phenyl-C₁₋₃ alkylene, and 5-6 membered heteroaryl-C₁₋₃ alkylene are each optionally substituted with 1, 2, 3, or 4 substituents independently selected from R¹²; each Rᵃ⁴, Rᶜ⁴, and Rᵈ⁴ is independently selected from H, C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₁₋₆ haloalkyl, cycloalkyl |
| priorityDate | 2018-09-25-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
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Total number of triples: 31.