http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-110425-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/A61K2039-55511 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D519-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D413-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-454 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P37-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/G01N33-5026 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/G01N33-5008 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D263-57 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/G01N33-6893 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/G01N33-5011 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D413-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P31-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D213-81 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-437 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D471-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P37-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K39-39 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-424 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K45-06 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D471-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-437 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P35-00 |
| filingDate | 2017-12-21-04:00^^<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_034946872d65b433059c2e632d043086 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_1592e1f0f33992b94bd54e0c2a96aa44 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_46eebff0f1d1f0240b35dd0b662ec283 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_d7ff4284a8c12a8a116cdbf468a922ea http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_7fe4db3270a454af0ff0fee6dd96c694 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_f2d9c268ae7fda7be39dfa980054b044 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_0619e924d32d7b1fb7c1ef8c7d2901a0 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_ffa4d625ba7b593716e19cc5b63c82be http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_666266e67548dc925fed56b83eb8a5d1 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_e5aa9adb79b91cc60a0082ed1f17b426 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_1be5fde8c6bc6718a316972ec99eed3e http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_138058beece131c9f9381c7d694a3c26 |
| publicationDate | 2019-03-27-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-110425-A1 |
| titleOfInvention | IMMUNOMODULATING COMPOUNDS AND THEIR USE IN THE TREATMENT OF DISEASES RELATED TO PD-1 |
| abstract | Compositions and methods for inducing internalization of PD-L1 are described. The methods include reducing the amount of PD-L1 of the cell surface by contacting a cell that expresses PD-L1 with a compound that binds to the PD-L1 of the cell surface and induces the internalization of PD-L1. Compounds that induce internalization of PD-L1 can be used to enhance, stimulate and / or increase an immune response and treat a disease or condition related to PD-1. Claim 39: A compound of formula (1), or a pharmaceutically acceptable salt or a stereoisomer thereof, wherein: ring A is 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C₆₋₁₀ aryl or C₃₋₁₀ cycloalkyl, wherein the heteroaryl of between 5 and 14 and the heterocycloalkyl of between 4 and 14 members have 1-4 heteroatoms as ring members selected from B, P, N, O and S, where the N atom , P or S as ring members are optionally oxidized and one or more carbon atoms as ring members are optionally replaced by a carbonyl group; and wherein ring A is optionally substituted with 1, 2, 3, 4 or 5 R²⁰ substituents; L is a bond, -NH-, -O-, -C (O) NH-, -C (= S) NH-, -C (= NH) NH-, -C (= NOH) NH-, -C (= NCN) NH-, -CH₂O- or -OCH₂-, where the carbonyl group on the -C (O) NH- bond is attached to ring A; R²¹ and R²² are independently halo, C₁₋₆ or CN alkyl; R²³ is H, C₁₋₆ alkyl or C₁₋₆ haloalkyl; R²⁵ is C₁₋₄ alkyl, C₁₋₄ alkoxy, C₁₋₄ haloalkyl, C₁₋₄ haloalkoxy, CN, halo, OH, -COOH, NH₂, -NHC₁₋₄ alkyl or -N (C₁₋₄ alkyl) ₂; R²⁶ is C₁₋₄ alkyl, C₁₋₄ alkoxy, C₁₋₄ haloalkyl, C₁₋₄ haloalkoxy, CN, halo, OH, -COOH, NH₂, -NHC₁₋₄ alkyl or -N (C₁₋₄ alkyl) ₂; R²⁴ is selected from H, C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₁₋₆ haloalkyl, C₁₋₆ haloalkoxy, C₆₋₁₀ aryl, C₃₋₁₄ cycloalkyl, 5-14 membered heteroaryl, heterocycloalkyl of 4-14 members, C₆₋₁₀-aryl-C₁₋₄-alkyl, C₃₋₁₄-cycloalkyl-C₁₋₄- alkyl, (5-14 membered heteroaryl) -C₁₋₄- alkyl, (4-14-membered heterocycloalkyl) -alkyl C₁₋₄, C₍O₎Rᵃ, C (O) NRᵃRᵃ, C (O) ORᵃ, C (= NRᵃ) Rᵃ, C (= NOH) Rᵃ, C (= NOH) NRᵃ, C (= NCN) NRᵃRᵃ, C (= NRᵃ) NRᵃRᵃ, S (O) Rᵃ, S (O) NRᵃRᵃ, S (O) ₂Rᵃ, -P (O) RᵃRᵃ, -P (O) (ORᵃ) (ORᵃ), -B (OH ) ₂, -B (ORᵃ) ₂ and S (O) ₂NRᵃRᵃ, where C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₆₋₁₀ aryl, C₃₋₁₄ cycloalkyl, 5-14 membered heteroaryl , 4-14 membered heterocycloalkyl, C₆₋₁₀-C₁₋₄-alkyl aryl, C₃₋₁₄-C₁₋₄- cycloalkyl, (heteroaryl of 5-14 members) -C₁₋₄ alkyl and (4-14 membered heterocycloalkyl) -C₁₋₄ alkyl of R²⁴ are optionally substituted with, 1, 2, 3, 4 or 5 independently selected Rᵇ substituents; R²⁰ is independently selected from H, halo, C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₁₋₆ haloalkyl, C₁₋₆ haloalkoxy, C₆₋₁₀ aryl, C₃₋₁₄ cycloalkyl, 5-14 membered heteroaryl , 4-14 membered heterocycloalkyl, C₆₋₁₀-aryl-C alquilo- alkyl, C₃₋₁₄-cycloalkyl-C₁₋₄- alkyl, (5-14 membered heteroaryl) -C₁₋₄- alkyl, (4 - heterocycloalkyl) 14 members) -C₁₋₄-, CN, NO₂, ORᵃ¹, SRᵃ¹, NHORᵃ¹, C (O) Rᵃ¹, C (O) NRᵃ¹Rᵃ¹, C (O) ORᵃ¹, C (O) NRᵃ¹S (O) ₂Rᵃ¹, OC ( O) Rᵃ¹, OC (O) NRᵃ¹Rᵃ¹, NHRᵃ¹, NRᵃ¹Rᵃ¹, NRᵃ¹C (O) Rᵃ¹, NRᵃ¹C (= NRᵃ¹) Rᵃ¹, NRᵃ¹C (O) ORᵃ¹, NRᵃ¹C (O) NRᵃ¹Rᵃ¹, C (= NRᵃ¹) Rᵃ¹, C (= NOH ) Rᵃ¹, C (= NOH) NRᵃ¹, C (= NCN) NRᵃ¹Rᵃ¹, NRᵃ¹C (= NCN) NRᵃ¹Rᵃ¹, C (= NRᵃ¹) NRᵃ¹Rᵃ¹, NRᵃ¹C (= NRᵃ¹) NRᵃ¹Rᵃ¹, NRᵃ¹S (O) Rᵃ¹, NRᵃ¹S (O) ₂Rᵃ¹, NRᵃ¹S (O) ₂NRᵃ¹Rᵃ¹, S (O) Rᵃ¹, S (O) NRᵃ¹R ᵃ¹, S (O) ₂Rᵃ¹, S (O) ₂NRᵃ¹C (O) Rᵃ¹, -P (O) Rᵃ¹Rᵃ¹, -P (O) (ORᵃ¹) (ORᵃ¹), -B (OH) ₂, -B (ORᵃ¹) ₂ and S (O) ₂NRᵃ¹Rᵃ¹, wherein C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₆₋₁₀ aryl, C₃₋₁₄ cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, aryl C₆₋₁₀-C₁₋₄ alkyl, C₃₋₁₄ cycloalkyl-C₁₋₄- alkyl, (5-14 membered heteroaryl) -C₁₋₄ alkyl- and (4-14 membered heterocycloalkyl) -C₁₋₄ alkyl R²⁰ are optionally substituted with 1, 2, 3, 4 or 5 independently selected Rᵇ substituents; R²⁷ is independently selected from H, halo, C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₁₋₆ haloalkyl, C₁₋₆ haloalkoxy, C₆₋₁₀ aryl, C₃₋₁₄ cycloalkyl, 5-14 membered heteroaryl , 4-14 membered heterocycloalkyl, C₆₋₁₀-aryl-C alquilo- alkyl, C₃₋₁₄-cycloalkyl-C₁₋₄- alkyl, (5-14 membered heteroaryl) -C₁₋₄- alkyl, (4 - heterocycloalkyl) 14 members) -alkyl C₁₋₄-, CN, NO₂, ORᵃ², SRᵃ², NHORᵃ², C (O) Rᵃ², C (O) NRᵃ²Rᵃ², C (O) ORᵃ², C (O) NRᵃ²S (O) ₂Rᵃ², OC ( O) Rᵃ², OC (O) NRᵃ²Rᵃ², NHRᵃ², NRᵃ²Rᵃ², NRᵃ²C (O) Rᵃ², NRᵃ²C (= NRᵃ²) Rᵃ², NRᵃ²C (O) ORᵃ², NRᵃ²C (O) NRᵃ²Rᵃ², C (= NRᵃ²) Rᵃ², C (= NOH ) Rᵃ², C (= NOH) NRᵃ², C (= NCN) NRᵃ²Rᵃ², NRᵃ²C (= NCN) NRᵃ²Rᵃ², C (= NRᵃ²) NRᵃ²Rᵃ², NRᵃ²C (= NRᵃ²) NRᵃ²Rᵃ², NRᵃ²S (O) Rᵃ², NRᵃ²S (O) ₂Rᵃ², O) NRᵃ²S (O) ₂NRᵃ²Rᵃ², S (O) Rᵃ², S (O) NRᵃ²R ᵃ², S (O) ₂Rᵃ², S (O) ₂NRᵃ²C (O) Rᵃ², -P (O) Rᵃ²Rᵃ², -P (O) (ORᵃ²) (ORᵃ²), B (OH) ₂, -B (ORᵃ²) ₂ and S (O) ₂NRᵃ²Rᵃ², where to C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₆₋₁₀ aryl, C₃₋₁₄ cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C₆ aryl ₋₁₀-C₁₋₄-alkyl, C₃₋₁₄-cycloalkyl-C₁₋₄-alkyl, (5-14 membered heteroaryl) -C₁₋₄-alkyl and (4-14-membered heterocycloalkyl) -C₁₋₄-alkyl R²⁷ are optionally substituted with 1, 2, 3, 4 or 5 independently selected Rᵇ substituents; or two R²⁰ substituents attached to the same carbon atom of the ring taken together with the carbon atom of the ring to which they form form C₃₋₆ spiro cycloalkyl or 4 to 7 spiro heterocycloalkyl, each of which is optionally substituted with 1, 2 or 3 independently selected Rᶠ substituents; or two R²⁷ substituents attached to the same carbon atom of the ring taken together with the carbon atom of the ring to which they form form C₃₋₆ spiro cycloalkyl or 4 to 7 spiro heterocycloalkyl, each of which is optionally substituted with 1, 2 or 3 independently selected Rᶠ substituents; each of Rᵃ, Rᵃ¹ and Rᵃ² is independently selected from H, C₁₋₆ alkyl, C₁₋₆ haloalkyl, C₂₋₆ alkenyl C₂₋₆ alkynyl, C₆₋₁₀ aryl, C₃₋₁₄ cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C₆₋₁₀-aryl-C alquilo- alkyl, C₃₋₁₄-cycloalkyl-C₁₋₄- alkyl, (5-14 membered heteroaryl) -C₁₋₄- alkyl and (4-14 heterocycloalkyl) members) -C₁₋₄ alkyl-, wherein C₁₋₄ alkyl, C₂₋₄ alkenyl, C₁₋₄ alkynyl, C₆₋₁₀ aryl, C₃₋₁₄ cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl , C₆₋₁₀-C₁₋₄-alkyl-, C₃₋₁₄-cycloalkyl-C₁₋₄- alkyl, (5-14 membered heteroaryl) -C₁₋₄- alkyl and (4-14 membered heterocycloalkyl) -C₁₋ alkyl ₄- of Rᵃ, Rᵃ¹ and Rᵃ² are optionally substituted- with 1, 2, 3, 4 or 5 independently selected Rᵈ substituents recently each Rᵈ is independently selected from C₁₋₆ alkyl, C₁₋₄ haloalkyl, halo, C₆₋₁₀ aryl, 5-14 membered heteroaryl, C₃₋₁₀ cycloalkyl, 4-14 membered heterocycloalkyl, C₁₋₄ aryl-C alquilo alkyl ₄, C₃₋₁₄-C₁₋₄- cycloalkyl, (5-14 membered heteroaryl) -C₁₋₄- alkyl (4-14 membered heterocycloalkyl) -C₁₋₄-, CN, NH₂, NHORᵉ, ORᵉ alkyl , SRᵉ, C (O) Rᵉ, C (O) NRᵉRᵉ, C (O) ORᵉ, C (O) NRᵉS (O) ₂Rᵉ, OC (O) Rᵉ, OC (O) NRᵉRᵉ, NHRᵉ, NRᵉRᵉ, NRᵉC (O ) Rᵉ, NRᵉC (= NRᵉ) Rᵉ, NRᵉC (O) NRᵉRᵉ, NRᵉC (O) ORᵉ, C (= NRᵉ) NRᵉRᵉ, NRᵉC (= NRᵉ) NRᵉRᵉ, NRᵉC (= NOH) NRᵉRᵉ, NRᵉC (= NCN) NRᵉRᵉ, S (O) Rᵉ, S (O) NRᵉRᵉ, S (O) ₂Rᵉ, S (O) ₂NRᵉC (O) Rᵉ, NRᵉS (O) ₂Rᵉ, NRᵉS (O) ₂NRᵉRᵉ, -P (O) RᵉRᵉ, -P ( O) (ORᵉ) (ORᵉ), -B (OH) ₂, -B (ORᵉ) ₂ and S (O) ₂NRᵉRᵉ, where C₁₋₆ alkyl, C₁₋₆ haloalkyl, C₆₋₁₀ aryl, 5-heteroaryl - 14 miem bros, C₃₋₁₄ cycloalkyl, 4-14 membered heterocycloalkyl, C₆₋₁₀ aryl-C₁₋₄ alkyl-, C ciclo cycloalkyl- C alquilo alkyl-, (5-14 membered heteroaryl) -C₁₋₄ alkyl and (4-14 membered heterocycloalkyl) -C₁₋₄ -alkyl of Rᵈ are optionally substituted with 1, 2 or 3 independently selected Rᶠ substituents; each Rᵉ is independently selected from H, C₁₋₆ alkyl, C₁₋₆ haloalkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₆₋₁₀ aryl, C₃₋₁₆ cycloalkyl, 5-10 membered heteroaryl, 4-10 heterocycloalkyl members, C₆₋₁₀-aryl-C alquilo-alkyl, C₃₋₁₆-cycloalkyl-C₁₋₄-alkyl, (5-10-membered heteroaryl) -C₁₋₄ -alkyl and (4-10-membered heterocycloalkyl) -C₁ -alkyl ₋₄-, wherein C₁₋₆ alkyl, C₁₋₆ haloalkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₆₋₁₀ aryl, C₃₋₁₆ cycloalkyl, 5-10 membered heteroaryl, 4-10 membered heterocycloalkyl , C₆₋₁₀-C₁₋₄-alkyl-, C₃₋₁₆-cycloalkyl-C₁₋₄- alkyl, (5-10 membered heteroaryl) -C₁₋₄- alkyl and (4-10 membered heterocycloalkyl) -C₁₋ alkyl ₄- of Rᵉ are optionally substituted with 1, 2 or 3 independently selected Rᶠ substituents; each substituent Rᵇ is independently selected from halo, C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₁₋₆ haloalkyl C₁₋₆ haloalkoxy, C₆₋₁₀ aryl, C₃₋₁₄ cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C₆₋₁₀-C₁₋₄- alkyl, C₃₋₁₄-C₁₋₄- cycloalkyl, (5-14 membered heteroaryl) -C₁₋₄- alkyl, (4-14 heterocycloalkyl) members) -alkyl C₁₋₄-, CN, OH, NH₂, NO₂, NHORᶜ, ORᶜ, SRᶜ, C (O) Rᶜ, C (O) NRᶜRᶜ, C (O) ORᶜ, C (O) NRᶜS (O) ₂Rᶜ , OC (O) Rᶜ, OC (O) NRᶜRᶜ, C (= NOH) Rᶜ, C (= NOH) NRᶜ, C (= NCN) NRᶜRᶜ, NRᶜC (= NCN) NRᶜRᶜ, C (= NRᶜ) NRᶜRᶜ, NRᶜC ( = NRᶜ) NRᶜRᶜ, NHRᶜ, NRᶜRᶜ, NRᶜC (O) Rᶜ, NRᶜC (= NRᶜ) Rᶜ, NRᶜC (O) ORᶜ, NRᶜC (O) NRᶜRᶜ, NRᶜS (O) Rᶜ, NRᶜS (O) ₂Rᶜ, NRCS (O) ₂NRᶜRᶜ, S (O) Rᶜ, S (O) NRᶜRᶜ, S (O) ₂Rᶜ, S (O) ₂NRᶜC (O) Rᶜ, -P (O) RᶜRᶜ, -P (O) (ORᶜ) (ORᶜ), - B (OH) ₂, -B (OR ) ₂ and S (O) ₂NRᶜRᶜ; wherein C₁₋₆ alkyl, C₁₋₆ haloalkyl, C₁₋₆ haloalkoxy, C₁₋₆ alkenyl, C₁₋₆ alkynyl, C₆₋₁₀ aryl, C₃₋₁₄ cycloalkyl, 5-14 membered heteroaryl, 4-14 heterocycloalkyl members, C₆₋₁₀-aryl-C alquilo-alkyl, C₁₋₄-cycloalkyl-C₁₋₄-alkyl, (5-14 membered heteroaryl) -C₁₋₄ -alkyl and (4-14-membered heterocycloalkyl) -C₁ alkyl ₋₄- of Rᵇ are optionally further substituted with 1, 2 or 3 independently selected Rᵈ substituents; each Rᶜ is independently selected from H, C₁₋₆ alkyl, C₁₋₆ haloalkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₆₋₁₀ aryl, C₃₋₁₄ cycloalkyl, 5-14 membered heteroaryl, 4-14 heterocycloalkyl members, C₆₋₁₀-aryl-C alquilo-alkyl, C₃₋₁₄-cycloalkyl-C₁₋₄-alkyl, (5-14 membered heteroaryl) -C₁₋₄ -alkyl and (4-14-membered heterocycloalkyl) -C₁ alkyl ₋₄-, wherein C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₆₋₁₀ aryl, C₃₋₁₄ cycloalkyl, 5-14 membered heteroaryl, 4-14 membered heterocycloalkyl, C₆₋₁₀ aryl -C₁₋₄-alkyl, C₃₋₁₄-cycloalkyl-C₁₋₄-alkyl, (5-14 membered heteroaryl) -C₁₋₄-alkyl and (4-14-membered heterocycloalkyl) -C₁₋₄-alkyl of Rᶜ se optionally substituted with 1, 2, 3, 4 or 5 independently selected Rᶠ substituents; each Rᶠ is independently selected from C₁₋₆ alkyl, C₁₋₆ haloalkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₆₋₁₀ aryl, C₃₋₁₀ cycloalkyl, 5-10 membered heteroaryl, 4-10 membered heterocycloalkyl, C₆₋₁₀-aryl-C alquilo-alkyl, C₃₋₁₀-cycloalkyl-C₁₋₄-alkyl, (5-10 membered heteroaryl) -C₁₋₄- alkyl, (4-10 membered heterocycloalkyl) -C₁₋₄ alkyl -, halo, CN, NHORᵍ, ORᵍ, SRᵍ, C (O) Rᵍ, C (O) NRᵍRᵍ, C (O) ORᵍ, C (O) NRᵍS (O) ₂Rᵍ, OC (O) Rᵍ, OC (O) NRᵍRᵍ, NHRᵍ, NRᵍRᵍ, NRᵍC (O) Rᵍ, NRᵍC (= NRᵍ) Rᵍ, NRᵍC (O) NRᵍRᵍ, NRᵍC (O) ORᵍ, C (= NRᵍ) NRᵍRᵍ, NRᵍC (= NRᵍ) NRᵍRᵍ, S (O) Rᵍ , S (O) NRᵍRᵍ, S (O) ₂Rᵍ, S (O) ₂NRᵍC (O) Rᵍ, NRᵍS (O) ₂Rᵍ, NRᵍS (O) ₂NRᵍRᵍ, -P (O) RᵍRᵍ, -P (O) (ORᵍ) (ORᵍ), -B (OH) ₂, -B (ORᵍ) ₂ and S (O) ₂NRᵍRᵍ; wherein C₁₋₆ alkyl, C₁₋₆ haloalkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₆₋₁₀ aryl, C₃₋₁₀ cycloalkyl, 5-10 membered heteroaryl, 4-10 membered heterocycloalkyl, C₆₋ aryl ₁₀-C₁₋₄-alkyl, C₃₋₁₀-cycloalkyl-C₁₋₄-alkyl, (5-10 membered heteroaryl) -C₁₋₄-alkyl and (4-10-membered heterocycloalkyl) -C₁₋₄- alkyl of Rᶠ they are optionally substituted with 1, 2, 3, 4 or 5 independently selected Rⁿ substituents; each Rⁿ are substituents independently selected from C₁₋₆ alkyl, C₁₋₆ haloalkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₆₋₁₀ C₆₋₁₀ cycloalkyl, 5-10 membered heteroaryl, 4-10 membered heterocycloalkyl, C₆₋₁₀-aryl-C₁₋₄-alkyl, C₃₋₁₀-cycloalkyl-C₁₋₄-alkyl, (5-10 membered heteroaryl) -C₁₋₄-alkyl, (4-10-membered heterocycloalkyl) -C₁₋₄ alkyl, halo , CN, NHORᵒ, ORᵒ, SRᵒ, C (O) Rᵒ, C (O) NRᵒRᵒ, C (O) ORᵒ, C (O) NRᵒS (O) ₂Rᵒ, OC (O) Rᵒ, OC (O) NRᵒRᵒ, NHRᵒ , NRᵒRᵒ, NRᵒC (O) Rᵒ, NRᵒC (= NRᵒ) Rᵒ, NRᵒC (O) NRᵒRᵒ, NRᵒC (O) ORᵒ, C (= NRᵒ) NRᵒRᵒ, NRᵒC (= NRᵒ) NRᵒRᵒ, S (O) Rᵒ, S ( O) NRᵒRᵒ, S (O) ₂Rᵒ, S (O) ₂NRᵒC (O) Rᵒ, NRᵒS (O) ₂Rᵒ, NRᵒS (O) ₂NRᵒRᵒ, -P (O) RᵒRᵒ, - P (O) (ORᵒ) (ORᵒ) , -B (OH) ₂, -B (ORᵒ) ₂ and S (O) ₂NRᵒRᵒ, wherein the C₁₋₆ alkyl, C₁₋₆ haloalkyl, C₂₋₆ alkenyl, C₂ alkynyl ₆, C₆₋₁₀ aryl, C₃₋₁₀ cycloalkyl, 5-10 membered heteroaryl, 4-10 membered heterocycloalkyl, C₆₋₁₀ aryl-C alquilo alkyl, C₃₋₁₀ cycloalkyl-C₁₋₄ alkyl, (5-heteroaryl - 10 members) -C₁₋₄ alkyl and (4-10 membered heterocycloalkyl) -C₁₋₄ alkyl of Rⁿ are optionally substituted with 1, 2 or 3 independently selected Rq substituents; each Rᵍ is independently selected from H, C₁₋₆ alkyl, C₁₋₆ haloalkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₆₋₁₀ aryl, C₃₋₁₀ cycloalkyl, 5-10 membered heteroaryl, 4-10 heterocycloalkyl members, C₆₋₁₀-aryl-C alquilo-alkyl, C₃₋₁₀-cycloalkyl-C₁₋₄-alkyl, (5-10-membered heteroaryl) -C₁₋₄ -alkyl and (4-10-membered heterocycloalkyl) -C₁ -alkyl ₋₄-, wherein C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₆₋₁₀ aryl, C₃₋₁₀ cycloalkyl, 5-10 membered heteroaryl, 4-10 membered heterocycloalkyl, C₆₋₁₀ aryl -C₁₋₄-alkyl, C₃₋₁₀-cycloalkyl-C₁₋₄-alkyl, (5-10 membered heteroaryl) -C₁₋₄-alkyl and (4-10-membered heterocycloalkyl) -C₁₋₄-alkyl of Rᵍ se optionally substituted with 1, 2 or 3 independently selected Rᵖ substituents; each Rᵖ is independently selected from C₁₋₆ alkyl, C₁₋₆ haloalkyl, C₂₋₆ alkenyl, C₁₋₆ alkynyl, C₆₋₁₀ aryl, C₃₋₁₀ cycloalkyl, 5-10 membered heteroaryl, 4-10 membered heterocycloalkyl, C₆₋₁₀-aryl-C alquilo-alkyl, C₃₋₁₀-cycloalkyl-C₁₋₄- alkyl, (5-10 membered heteroaryl) -C₁₋₄ alkyl, (4-10 membered heterocycloalkyl) -C₁₋₄ alkyl , halo, CN, NHORʳ, ORʳ, SRʳ, C (O) Rʳ, C (O) NRʳRʳ, C (O) ORʳ, C (O) NRʳS (O) ₂Rʳ, OC (O) Rʳ, OC (O) NRʳRʳ , NHRʳ, NRʳRʳ, NRʳC (O) Rʳ, NRʳC (= NRʳ) Rʳ, NRʳC (O) NRʳRʳ, NRʳC (O) ORʳ, C (= NRʳ) NRʳRʳ, NRʳC (= NRʳ) NRʳRʳ, NRʳC (= NOH) NRʳRʳ , NRʳC (= NCN) -NRʳRʳ, S (O) Rʳ, S (O) NRʳRʳ, S (O) ₂Rʳ, S (O) ₂NRʳC (O) Rʳ, NRʳS (O) ₂Rʳ, NRʳS (O) ₂NRʳRʳ, - P (O) RʳRʳ, -P (O) (ORʳ) (ORʳ), -B (OH) ₂, -B (ORʳ) ₂ and S (O) ₂NRʳRʳ, where the C₁₋₆ alkyl, C₁₋₆ haloalkyl , C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₆₋₁ aryl , C₃₋₁₀ cycloalkyl, 5-10 membered heteroaryl, 4-10 membered heterocycloalkyl, C₆₋₁₀-C₁₋₄-aryl alkyl, C₃₋₁₀-C₁₋₄- cycloalkyl, (5-10 membered heteroaryl) -C₁₋₄ alkyl and (4-10 membered heterocycloalkyl) -C₁₋₄ alkyl of Rᵖ are optionally substituted with 1, 2 or 3 independently selected Rq substituents; or two Rᵃ substituents together with the boron, phosphorus or nitrogen atom to which they bind form a heterocycloalkyl group of 4, 5, 6, 7, 8, 9 or 10 members optionally substituted with 1, 2 or 3 independently selected Rʰ substituents; or two Rᵃ¹ substituents together with the boron, phosphorus or nitrogen atom to which they bind form a 4, 5, 6, 7, 8, 9 or 10-membered heterocycloalkyl group optionally substituted with 1, 2 or 3 independently selected Rʰ substituents; or two Rᵃ² substituents together with the boron, phosphorus or nitrogen atom to which they bind form a 4, 5, 6, 7, 8, 9 or 10-membered heterocycloalkyl group optionally substituted with 1, 2 or 3 independently selected Rʰ substituents; each Rʰ is independently selected from C₁₋₆ alkyl, C₃₋₁₀ cycloalkyl, 4-10 membered heterocycloalkyl, C₆₋₁₀ aryl, 5-10 membered heteroaryl, C₆₋₁₀ aryl-C₁₋₄- alkyl, C₃₋₁₀ cycloalkyl -C₁₋₄ alkyl, (5-10 membered heteroaryl) -C₁₋₄ alkyl, (4-10 membered heterocycloalkyl) -C₁₋₄ alkyl, C₁₋₆ haloalkyl, C₁₋₆ haloalkoxy C₂₋₆ alkenyl, C₂ alkynyl ₋₆, halo, CN, ORⁱ, SRⁱ, NHORⁱ, C (O) Rⁱ, C (O) NRⁱRⁱ, C (O) ORⁱ, C (O) NRⁱS (O) ₂Rⁱ, OC (O) Rⁱ, OC (O ) NRⁱRⁱ, NHRⁱ, NRⁱRⁱ, NRⁱC (O) Rⁱ, NRⁱC (= NRⁱ) Rⁱ, NRⁱC (O) NRⁱRⁱ, NRⁱC (O) ORⁱ, C (= NRⁱ) NRⁱRⁱ, NRⁱC (= NRⁱ) NRⁱRⁱ, S (O) Rⁱ, S (O) NRⁱRⁱ, S (O) ₂Rⁱ, S (O) ₂NRⁱC (O) Rⁱ, NRⁱS (O) ₂Rⁱ, NRⁱS (O) ₂NRⁱRⁱ, -P (O) RⁱRⁱ, -P (O) (ORⁱ ) (ORⁱ), -B (OH) ₂, -B (ORⁱ) ₂ and S (O) ₂NRⁱRⁱ, where C₁₋₆ alkyl, C₂₋₆ alkenyl, C₁₋₆ alkynyl, C cycloalkyl ₃₋₁₀, 4-10 membered heterocycloalkyl, C₆₋₁₀ aryl, 5-10 membered heteroaryl, C₆₋₁₀ aryl-C alquilo alkyl, C₃₋₁₀ cycloalkyl-C alquilo alkyl, (5-10 membered heteroaryl ) -C₁₋₄ alkyl and (4-10 membered heterocycloalkyl) -C₁₋₄ alkyl of Rʰ are optionally substituted by 1, 2 or 3 independently selected Rʲ substituents; each Rʲ is independently selected from C₃₋₆ cycloalkyl, C₆₋₁₀ aryl, 5- or 6-membered heteroaryl, 4-7 membered heterocycloalkyl, C₂₋₄ alkenyl, C₂₋₄ alkynyl, halo, C₁₋₄ alkyl, haloalkyl |
| priorityDate | 2016-12-22-04:00^^<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: 52.