http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-114003-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_00f9e79ee7f3165c1cd1276c7a296e92 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D417-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-519 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-517 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D405-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D405-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D239-88 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D409-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D403-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D471-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D413-14 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D405-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D403-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D239-74 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P29-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-517 |
| filingDate | 2018-12-20-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_ff932ade7353f191b6c5661e50469e00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_5958febdf2677b0d79d7edc9a81abbe9 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_22fbf25748b3abddbf20aadf5c884990 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_f55ddbba1b4ab2137fc49ec68a239750 |
| publicationDate | 2020-07-08-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-114003-A1 |
| titleOfInvention | QUINAZOLINONES AS PARP14 INHIBITORS |
| abstract | Quinazolinones and related compounds which are inhibitors of PARP14 and are useful, for example, in the treatment of cancer and inflammatory diseases. Claim 1: A compound characterized in that it is of formula (1), or a pharmaceutically acceptable salt thereof, where: W is CRW or N; X is CRX or N; Y is CRY or N; Z is CRZ or N; where no more than two of W, X, Y and Z are simultaneously N; Ring A is C₃₋₁₄ monocyclic or polycyclic cycloalkyl or Ring A is 4-18 membered monocyclic or polycyclic heterocycloalkyl, where Ring A is optionally substituted with 1, 2, 3, or 4 RA, and Ring A is attached to the - (L) ₘ- unit of formula (1) through a non-aromatic ring when Ring A is polycyclic; L is - (CR⁵R⁶) ₜ-, - (CR⁵R⁶) ₚ-O- (CR⁵R⁶) q-, - (CR⁵R⁶) ₚ-S- (CR⁵R⁶) q-, - (CR⁵R⁶) ₚ-NR³- (CR⁵R⁶) q- , - (CR⁵R⁶) ₚ-CO- (CR⁵R⁶) q-, - (CR⁵R⁶) ʳ-C (O) O- (CR⁵R⁶) ₛ-, - (CR⁵R⁶) ʳ-CONR³- (CR⁵R⁶) ₛ-, - (CR⁵R⁶ ) ₚ-SO- (CR⁵R⁶) q-, - (CR⁵R⁶) ₚ-SO₂- (CR⁵R⁶) q-, - (CR⁵R⁶) ʳ-SONR³- (CR⁵R⁶) ₛ-, or -NR³CONR⁴-; R¹ and R² are independently selected from H and methyl; R³ and R⁴ are independently selected from H and C₁₋₄ alkyl; R⁵ and R⁶ are independently selected from H, halo, C₁₋₄ alkyl, C₁₋₄ alkoxy, C₁₋₄ haloalkyl, amino, C₁₋₄ alkylamino, and C₂₋₈ dialkylamino; each RA is independently selected from halo, C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₁₋₆ haloalkyl, C₆₋₁₀ aryl, C₃₋₇ cycloalkyl, 5-10 membered heteroaryl, 4-4 heterocycloalkyl - 10 membered, C₆₋₁₀ aryl-C₁₋₄ alkyl, C₃₋₇ cycloalkyl-C₁₋₄ alkyl, 5-10 membered heteroaryl-C₁₋₄ alkyl, 4-10 membered heterocycloalkyl-C₁₋₄ alkyl, 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 (= 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, C₁₋₆ haloalkyl, C₆₋₁₀ aryl, C₃₋₇ cycloalkyl, 5-10 membered heteroaryl, 4-10 membered heterocycloalkyl, C₆₋₁₀ aryl -C₁₋₄ alkyl, C₃₋₇ cycloalkyl-C₁₋₄ alkyl, 5-10 membered heteroaryl-C₁₋₄ alkyl, and 4-10 membered heterocycloalkyl-C₁₋₄ alkyl of RA are optionally substituted with 1, 2, 3, 4 or 5 substituents independently selected from Cy¹, Cy¹-C₁₋₄ alkyl, halo, C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₁₋₆ haloalkyl, CN, NO₂, ORᵃ¹, SRᵃ¹, C (O) Rᵇ¹, C (O) NRᶜ¹Rᵈ¹, C (O) ORᵃ¹, OC (O) Rᵇ¹, OC (O) NRᶜ¹Rᵈ¹, C (= NRᵉ¹) NRᶜ¹Rᵈ¹, NRᶜ¹C (= NRᵉ¹) NRᶜ¹Rᵈ¹, NRᶜ¹Rᵈ¹, NRᶜ¹C (O) Rᵇ¹, NRᶜ¹C (O) ORᵃ¹, NRᶜ¹C (O) NRᶜ¹Rᵈ¹, NRᶜ¹S (O) Rᵇ¹, NRᶜ¹S (O) ₂Rᵇ¹, NRᶜ¹S (O) ₂NRᶜ¹Rᵈ¹, S (O) Rᵇ¹, S (O) NRᶜ¹Rᵈ¹, S (O) ₂Rᵇ¹, and S (O) ₂NRᶜ¹Rᵈ¹; RW, RX, RY, and RZ are independently selected from H, halo, C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₁₋₆ haloalkyl, C₆₋₁₀ aryl, C₃₋₇ cycloalkyl, heteroaryl of 5-10 membered, 4-10 membered heterocycloalkyl, C₆₋₁₀ aryl-C₁₋₄ alkyl, C₃₋₇ cycloalkyl-C₁₋₄ alkyl, 5-10 membered heteroaryl-C₁₋₄ alkyl, heterocycloalkyl-C₁₋₄ alkyl 4-10 membered, 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 (= NRᵉ²) NRᶜ²Rᵈ², NRᶜ²C (= NRᵉ²) NRᶜ²Rᵈ², NRᶜ²S (O) R²², NRᶜᶜS (O) R²², NRᶜR² ) 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, C₁₋₆ haloalkyl, C₆₋₁₀ aryl, C₃₋₇ cycloalkyl, 5-10 membered heteroaryl, 4-10 membered heterocycloalkyl, C₆₋₁₀ aryl -C₁₋₄ alkyl, C₃₋₇ cycloalkyl-C₁₋₄ alkyl, 5-10 membered heteroaryl-C₁₋₄ alkyl, and 4-10 membered heterocycloalkyl-C₁₋₄ alkyl of RW, RX, RY, or RZ are optionally substituted with 1, 2, 3, 4, or 5 substituents independently selected from Cy², Cy²-C₁₋₄ alkyl, halo, C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₁₋₆ haloalkyl, CN , NO₂, ORᵃ², SRᵃ², C (O) Rᵇ², C (O) NRᶜ²Rᵈ², C (O) ORᵃ², OC (O) Rᵇ², OC (O) NRᶜ²Rᵈ², C (= NRᵉ²) NRᶜ²Rᵈ², NRᶜ²C (= NRᵉ²) NRᶜ²Rᵈ² , NRᶜ²Rᵈ², NRᶜ²C (O) Rᵇ², NRᶜ²C (O) ORᵃ², NRᶜ²C (O) NRᶜ²Rᵈ², NRᶜ²S (O) Rᵇ², NRᶜ²S (O) ₂Rᵇ², NRᶜ²S (O) ₂NRᶜ²Rᵈ², S (S (O) ₂NRᶜ²Rᵈ²), S (O () ₂NRᶜ²Rᵈ²) , S (O) ₂Rᵇ², and S (O) ₂NRᶜ²Rᵈ²; where if W is CRW, X is CRX, Y is CRY, and Z is CRZ, then at least one of RW, RX, RY, and RZ is not H; each Cy¹ is independently selected from C₆₋₁₀ aryl, C₃₋₇ cycloalkyl, 5-10 membered heteroaryl, and 4-10 membered heterocycloalkyl, each optionally substituted with 1, 2, 3, or 4 independently selected substituents halo, C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₁₋₆ haloalkyl, C₆₋₁₀ aryl-C₁₋₄ alkyl, C₃₋₇ cycloalkyl-C₁₋₄ alkyl, heteroaryl-C₁₋₄ alkyl of 5-10 membered, heterocycloalkyl-C₁₋₄ 4-10 membered alkyl, CN, NO₂, ORᵃ¹, SRᵃ¹, C (O) Rᵇ¹, C (O) NRᶜ¹Rᵈ¹, C (O) ORᵃ¹, OC (O) Rᵇ¹, OC (O) NRᶜ¹Rᵈ¹, C (= NRᵉ¹) NRᶜ¹Rᵈ¹, NRᶜ¹C (= NRᵉ¹) NRᶜ¹Rᵈ¹, NRᶜ¹Rᵈ¹, NRᶜ¹C (O) Rᵇ¹, NRᶜ¹C (O) ORᵃ¹, NRᶜ¹C (O) NRᶜ¹Rᵈ¹, NRᶜ¹S (O) Rᵇ¹, NRᶜ¹S (O) ₂Rᵇ¹ , NRᶜ¹S (O) ₂NRᶜ¹Rᵈ¹, S (O) Rᵇ¹, S (O) NRᶜ¹Rᵈ¹, S (O) ₂Rᵇ¹, and S (O) ₂NRᶜ¹Rᵈ¹; Each Cy² is independently selected from C₆₋₁₀ aryl, C₃₋₇ cycloalkyl, 5-10 membered heteroaryl, and 4-10 membered heterocycloalkyl, each optionally substituted with 1, 2, 3, or 4 independently selected substituents halo, C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₁₋₆ haloalkyl, C₆₋₁₀ aryl-C₁₋₄ alkyl, C₃₋₇ cycloalkyl-C₁₋₄ alkyl, heteroaryl-C₁₋₄ alkyl of 5 - 10 membered, 4-10 membered heterocycloalkyl-C₁₋₄ alkyl, CN, NO₂, ORᵃ², SRᵃ², C (O) Rᵇ², C (O) NRᶜ²Rᵈ², C (O) ORᵃ², OC (O) Rᵇ², OC (O) NRᶜ²Rᵈ², C (= NRᵉ²) NRᶜ²Rᵈ², NRᶜ²C (= NRᵉ²) NRᶜ²Rᵈ², NRᶜ²Rᵈ², NRᶜ²C (O) Rᵇ², NRᶜ²C (O) ORᵃ², NRᶜ²C (O) NRᶜ²Rᵇ, NR₂²C (O) NR²RᵇS (NR²R²) , NRᶜ²S (O) ₂NRᶜ²Rᵈ², S (O) Rᵇ², S (O) NRᶜ²Rᵈ², S (O) ₂Rᵇ², and S (O) ₂NRᶜ²Rᵈ²; each Rᵃ¹, Rᵇ¹, Rᶜ¹, Rᵈ¹, Rᵃ², Rᵇ², Rᶜ², and Rᵈ² is independently selected from H, C₁₋₆ alkyl, C₁₋₆ haloalkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₆₋₁₀ aryl, C₃₋₇ cycloalkyl, 5-10 membered heteroaryl, 4-10 membered heterocycloalkyl, C₆₋₁₀ aryl-C₁₋₄ alkyl, C₃₋₇ cycloalkyl-C₁₋₄ alkyl, 5-10 membered heteroaryl-C₁₋₄ alkyl , and 4-10 membered heterocycloalkyl-C₁₋₄ alkyl, wherein said C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₆₋₁₀ aryl, C₃₋₇ cycloalkyl, 5-10 membered heteroaryl, heterocycloalkyl of 4-10 membered, C₆₋₁₀ aryl-C₁₋₄ alkyl, C₃₋₇ cycloalkyl-C₁₋₄ alkyl, 5-10 membered heteroaryl-C₁₋₄ alkyl, and 4-10 membered heterocycloalkyl-C₁₋₄ alkyl of Rᵃ¹, Rᵇ¹, Rᶜ¹, Rᵈ¹, Rᵃ², Rᵇ², Rᶜ², or Rᵈ² are optionally substituted with 1, 2, 3, 4, or 5 substituents independently selected from Cy³, Cy³-C₁₋₄ alkyl, halo, C₁₋₄ alkyl , C₁₋₄ haloalkyl, C₁₋₆ haloalkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, CN, ORᵃ³, S Rᵃ³, C (O) Rᵇ³, C (O) NRᶜ³Rᵈ³, C (O) ORᵃ³, OC (O) Rᵇ³, OC (O) NRᶜ³Rᵈ³, NRᶜ³Rᵈ³, NRᶜ³C (O) Rᵇ³, NRᶜ³C (O) NRᶜ³Rᵈ³, NRᶜ³C (O) ORᵃ³, C (= NRᵉ³) NRᶜ³Rᵈ³, NRᶜ³C (= NRᵉ³) NRᶜ³Rᵈ³, S (O) Rᵇ³, S (O) NRᶜ³Rᵈ³, S (O) ₂Rᵇ³, NRᶜ³S (O) ₂Rᵇ³, NRᶜ³S (O) ₂NR³, and NRᶜ³S (O) ₂NR³ ) ₂NRᶜRᵈ³; each Cy³ is C₆₋₁₀ aryl, C₃₋₇ cycloalkyl, 5-10 membered heteroaryl, or 4-10 membered heterocycloalkyl, each optionally substituted with 1, 2, 3, or 4 substituents independently selected from halo, C₁₋ ₄ alkyl, C₁₋₄ haloalkyl, C₁₋₆ haloalkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, CN, ORᵃ³, SRᵃ³, C (O) Rᵇ³, C (O) NRᶜ³Rᵈ³, C (O) ORᵃ³, OC (O ) Rᵇ³, OC (O) NRᶜ³Rᵈ³, NRᶜ³Rᵈ³, NRᶜ³C (O) Rᵇ³, NRᶜ³C (O) NRᶜ³Rᵈ³, NRᶜ³C (O) ORᵃ³, C (= NRᵉ³) NRᶜ³Rᵈ³, NRᶜ³C (= NRᵉ³) Rᵈ, S (O) NRᶜ³Rᵈ³, S (O) ₂Rᵇ³, NRᶜ³S (O) ₂Rᵇ³, NRᶜ³S (O) ₂NRᶜ³Rᵈ³, and S (O) ₂NRᶜ³Rᵈ³; Rᵃ³, Rᵇ³, Rᶜ³, and Rᵈ³ are independently selected from H, C₁₋₆ alkyl, C₁₋₆ haloalkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₆₋₁₀ aryl, C₃₋₇ cycloalkyl, 5-10 heteroaryl members, 4-10 membered heterocycloalkyl, C₆₋₁₀ aryl-C₁₋₄ alkyl, C₃₋₇ cycloalkyl-C₁₋₄ alkyl, 5-10 membered heteroaryl-C₁₋₄ alkyl, and 4-membered heterocycloalkyl-C₁₋₄ alkyl - 10 members, wherein said C₁₋₆ alkyl, C₁₋₆ haloalkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₆₋₁₀ aryl, C₃₋₇ cycloalkyl, 5-10 membered heteroaryl, 4-10 membered heterocycloalkyl, C₆₋₁₀ aryl-C₁₋₄ alkyl, C₃₋₇ cycloalkyl-C₁₋₄ alkyl, heteroaryl-C₁₋₄ alkyl, heteroaryl-C₁₋₄ 5-10 membered alkyl, and 4-10 heterocycloalkyl-C₁₋₄ alkyl members are optionally substituted with 1, 2, or 3 substituents independently selected from OH, CN, amino, halo, C₁₋₆ alkyl, C₁₋₆ alkoxy, C₁₋₆ haloalkyl, and C₁₋₆ haloalkoxy; or Rᶜ¹ and Rᵈ¹ together with the N atom to which they are attached form a 4-7 membered heterocycloalkyl group optionally substituted with 1, 2 or 3 substituents independently selected from halo, C₁₋₄ alkyl, C₁₋₄ haloalkyl, CN , ORᵃ³, SRᵃ³, C (O) Rᵇ³, C (O) NRᶜ³Rᵈ³, C (O) ORᵃ³, OC (O) Rᵇ³, OC (O) NRᶜ³Rᵈ³, NRᶜ³Rᵈ³, NRᶜ³C (O) Rᵇ³, NRᶜ³C (O) NRᶜ³Rᵈ³, NRᶜC (O) NRᶜ³Rᵈ³ (O) ORᵃ³, C (= NRᵉ³) NRᶜ³Rᵈ³, NRᶜ³C (= NRᵉ³) NRᶜ³Rᵈ³, S (O) Rᵇ³, S (O) NRᶜ³Rᵈ³, S (O) ₂Rᵇ³, NRᶜ³S (O) ₂R³³, NRᶜ³S (O) ₂R³³, NRᶜ³S (O) S (O) ₂NRᶜ³Rᵈ³; or Rᶜ² and Rᵈ² together with the N atom to which they are attached form a 4-7 membered heterocycloalkyl group optionally substituted with 1, 2 or 3 substituents independently selected from halo, C₁₋₄ alkyl, C₁₋₄ haloalkyl, CN , ORᵃ³, SRᵃ³, C (O) Rᵇ³, C (O) NRᶜ³Rᵈ³, C (O) ORᵃ³, OC (O) Rᵇ³, OC (O) NRᶜ³Rᵈ³, NRᶜ³Rᵈ³, NRᶜ³C (O) Rᵇ³, NRᶜ³C (O) NRᶜ³Rᵈ³, NRᶜC (O) NRᶜ³Rᵈ³ (O) ORᵃ³, C (= NRᵉ³) NRᶜ³Rᵈ³, NRᶜ³C (= NRᵉ³) NRᶜ³Rᵈ³, S (O) Rᵇ³, S (O) NRᶜ³Rᵈ³, S (O) ₂Rᵇ³, NRᶜ³S (O) ₂R³³, NRᶜ³S (O) ₂R³³, NRᶜ³S (O) S (O) ₂NRᶜ³Rᵈ³; each Rᵉ¹, Rᵉ², and Rᵉ³ is independently selected from H, C₁₋₄ alkyl, and CN; m is 0 or 1, n is 0, 1 or 2; p is 0, 1 or 2; q is 0, 1 or 2, where p + q is 0, 1 or 2; r is 0 or 1; s is 0 or 1, where r + s is 0 or 1; and t is 1, 2, or 3; wherein any heteroaryl or heterocycloalkyl group mentioned above comprises 1, 2, 3 or 4 heteroatoms forming part of the ring independently selected from O, N and S; where one or more C or N atoms forming part of the ring of any heterocycloalkyl group mentioned above are optionally substituted with an oxo group (= O); where one or more S atom forming part of the ring of any heterocycloalkyl group mentioned above are optionally substituted with one or two oxo groups (= O); where if W is CRW, X is CRX, Y is CRY and Z is CRZ and if m is 1 or 2, then RX and RY are not both methoxy; where the compound is not a compound selected from the group of formulas (2). |
| priorityDate | 2017-12-21-04:00^^<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: 44.