http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-111485-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_40765ca9a78b54a8a76f781d159ad145 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D413-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D417-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4353 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C57-24 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D487-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-438 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P35-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4427 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-12 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/C07D471-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D403-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D471-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D213-84 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D409-12 |
| filingDate | 2018-04-20^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_9150f9a375c7b176c1933cd7419e2717 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_20e620f9db1402391b53d8597b607844 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_3aca3eb9cc00227a75d0020199a76701 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_b4f0586ab44b7b4f41a541d5dddc1cb2 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_d15259c22e8288338de35dec91c24a69 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_6928d8a4792fe0dda19e4c22a6e30f07 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_7cf4907d039cbd3621ecbadb67895d07 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_b9f7cb8489583b5d4c02177d6d4e4c94 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_e7ead8220e673ed3f7b4835faf1e3d31 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_c14940014a6aa397e304272c68a2bf8a http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_38612ba45d4186cdedbdbf1eb4f94702 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_0701a26bc345ddaf99f0c8589da65284 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_e28acfc2761c6f94c2421ce6203aa153 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_bfa6cd85b20747fbde201d9c9d465b7a http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_26bc73313581de05a711a7f81fc4b5e4 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_fa0a8872685ab6f24e756d9423e612df http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_86d5495dd9b4e1132ce4a2f49b6d8067 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_850a329a7cf7a8e0362187d34f43d449 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_4241d89f4a711690275aa5f6e4c97d69 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_807cc63d935a7cffda0b74801ac5c94a http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_38ff9847e681b10ceac527858d145cc9 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_41ce955490e685b6c5d8c7e4a7fe8ed4 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_ad691877ad3667a78fb7dc809484686d http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_44674cda962a43d4d7d0619e8155faa6 |
| publicationDate | 2019-07-17^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-111485-A1 |
| titleOfInvention | PD-1 / PD-L1 INHIBITORS |
| abstract | Claim 1: A compound of formula (1), wherein: each of X⁴ and X⁵ are independently N, CH or CZ³; each Z¹ is independently halo, -ORᵃ, -NO₂, -CN, -NRᵃRᵇ, -N₃, -SO₂Rᵃ, -C₁₋₆ alkyl, -haloalkyl C₁₋₆, -C₂₋₆ alkenyl, -C₂₋₆ alkynyl, -O -C₁₋₆ alkyl, -O-C₁₋₆ haloalkyl, -C₃₋₈ cycloalkyl, or -C₁₋₆ -cycloalkyl alkyl; and wherein each alkyl, alkenyl, alkynyl and cycloalkyl is optionally substituted with 1 to 4 groups independently selected from oxo, -NO₂, -N₃, -ORᵃ, halo and cyano; each w is independently 0, 1 or 2; each Z³ is independently halo, -ORᵃ, -N₃, -NO₂, -CN, -NR¹R², -SO₂Rᵃ, -SO₂NRᵃRᵇ, -NRᵃSO₂Rᵃ, -NRᵃC (O) Rᵃ, -C (O) Rᵃ, -C (O) ORᵃ , -C (O) NRᵃRᵇ, -NRᵃC (O) ORᵃ, -NRᵃC (O) NR¹R², -OC (O) NRᵃRᵇ, -NRᵃSO₂NRᵃRᵇ, -C (O) NRᵃSO₂NRᵃRᵇ, -alkyl C₁₋₆, -alkenyl C₂₋₆ , -C₂₋₆ -alkynyl, -O-C₁₋₆-alkyl, -C₃₋₈ -cycloalkyl, -C₁₋₆ -alkyl-C₃₋₈ -alkyl, aryl, heteroaryl, heterocyclyl and RN; and wherein the alkyl, alkenyl, alkynyl, C₃₋₈ cycloalkyl, aryl, heteroaryl or heterocyclyl group is optionally substituted with 1 to 4 groups independently selected from oxo, -NO₂, -N₃, -ORᵃ, halo, cyano, -NRᵃRᵇ, -C (O) Rᵃ, -C (O) ORᵃ, -O-cyanoalkyl C₁₋₆, -C (O) NRᵃRᵇ, NRᵃC (O) Rᵃ, -NRᵃC (O) ORᵃ, -SO₂Rᵃ, -NRᵃSO₂Rᵇ, -SO₂NRᵃRᵇ , -NRᵃSO₂NRᵃRᵇ, -C (O) NRᵃSO₂NRᵃRᵇ and -C₃₋₈ -cycloalkyl; and additionally where the heteroaryl or heterocyclic group can be oxidized in a nitrogen atom to form an N-oxide or it can be oxidized in a sulfur atom to form a sulfoxide or sulfone; RN is independently -C₁₋₆NR¹R² alkyl, -O-C₁₋₆NR¹R² alkyl, -C₁₋₆C₁₋₆NR¹R² alkyl, -NRᵃ-C₁₋₆NR¹R² alkyl, -C₁₋₆C₍O₎NR¹R² alkyl, -O-C₁₋ alkyl ₆C₍O₎NR¹R², -O-C₁₋₆C₍O₎OR¹ alkyl, -S-C₁₋₆NR¹R² alkyl, -C₁₋₆ORᵃ alkyl, or a moiety of formula (2); wherein: L¹ is independently a link, O, NRᵃ, S, SO or SO₂; V is independently selected from a bond, C₁₋₆ alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynyl; wherein each alkyl, alkenyl or alkynyl is optionally independently substituted with ORᵃ, halo, cyano, -NRᵃRᵇ or -C₃₋₈ -cycloalkyl; L² is independently a bond, O, NRᵃ, S, SO or SO₂; Ring A is independently cycloalkyl, aryl, heteroaryl or heterocyclyl; wherein each cycloalkyl, aryl, heteroaryl or heterocyclyl is optionally substituted with 1 to 4 groups independently selected from oxo, -NO₂, -N₃, -ORᵃ, halo, cyano, -C₁₋₆ alkyl, -haloalkyl C₁₋₆, -alkenyl C₂₋₆, -C₂₋₆ alkynyl, -O-C₁₋₆ haloalkyl, NRᵃRᵇ, -C (O) Rᵃ, -C (O) ORᵃ, -O-C₁₋₆CN alkyl, -C (O) NRᵃRᵇ, - NRᵃC (O) Rᵃ, -NRᵃC (O) ORᵃ, -NRᵃC (O) ORᵃ, -C (O) N (Rᵃ) ORᵇ, -SO₂Rᵃ, -SO₂NRᵃRᵇ, -NRᵃSO₂Rᵇ, -NRᵃSO₂NRᵃRᵇ, -C (O) NRᵃSO₂NRᵃRᵇ, C₃₋₈ cycloalkyl, and C₁₋₆cycloalkyl alkyl; and wherein the alkyl, alkenyl or alkynyl group is optionally independently substituted with -ORᵃ, halo, cyano, -NRᵃRᵇ or -C₃₋₈ -cycloalkyl; each t is independently 0, 1 or 2; RE and RW are independently -NR¹R², C₁₋₆NR¹R² alkyl, -O-C₁₋₆NR¹R² alkyl, -C₁₋₆C₁₋₆NR¹R² alkyl, -NRᵃ-C₁₋₆NR¹R² alkyl, -C₁₋₆N⁺R¹R²R³ alkyl, -S-alkyl C₁₋₆NR¹R², -C (O) NR¹R², -SO₂Rᵃ, - (CH₂) ᵘSO₂NR¹R², - (CH₂) ᵘNRᵃ-SO₂NRᵃRᵇ, -SO₂NRᵃ-C₁₋₆NR¹R² alkyl, -NRᵃSO₂-C₁₋₆NR¹R² alkyl, - (CH₂) ᵘ O) NRᵃSO₂NRᵃRᵇ, - (CH₂) ᵘN⁺R¹R²O⁻, - (CH₂) ᵘP⁺RᵇRᶜRᵈ, - (CH₂) ᵘP⁺RᶜRᵈO⁻, (CH₂) ᵘP⁺O [NRᵃRᵇ] [NRᶜRᵈ], - (CH₂) ᵘNRᶜP (O ) (ORᶜ) ₂, - (CH₂) ᵘCH₂OP (O) (ORᶜ) (ORᵈ), - (CH₂) ᵘOP (O) (ORᶜ) (ORᵈ), - (CH₂) ᵘOP (O) (NRᵃRᵇ) (ORᵃ) , or a remainder of formula (3); wherein: V² is independently a bond, O, NRᵃ, S, SO, SO₂, C (O) NRᵃ, NRᵃC (O), SO₂NR¹, or NRᵃSO₂; L³ is independently a bond, O, NRᵃ, S, SO, SO₂, C (O) NRᵃ, NRᵃC (O), SO₂NR¹, or NRᵃSO₂; Ring B is independently cycloalkyl, aryl, heteroaryl or heterocyclyl; T is independently H, ORᵃ, (CH₂) qNR¹R², (CH₂) qNRᵃC (O) Rᶜ, or (CH₂) qC (O) Rᵉ; p is independently 0, 1, 2, 3, 4 or 5; q is independently 0, 1, 2, 3, 4 or 5; u is 0, 1, 2, 3 or 4; z is 0, 1, 2 or 3; and wherein the alkyl, cycloalkyl, aryl, heteroaryl or heterocyclyl of RE or RW is optionally substituted with 1 to 3 substituents independently selected from the group consisting of NRᵃRᵇ, halo, cyano, oxo, ORᵃ, -C₁₋₆ alkyl, -haloalkyl C₁₋₆, -C₁₋₆ -alkyl-alkyl, -C₁₋₆NRᵃRᵇ -alkyl, -C₁₋₆OH-alkyl, -C₃₋₈ -cycloalkyl, and -C₁₋₃ -C₃₋₈ -cycloalkyl; provided that at least one of V², L³, ring B and T contains a nitrogen atom; each R¹ is independently selected from H, -C₁₋₈ alkyl, -C₂₋₆ -alkenyl, -Cquin -alkyl, -C₃₋₆ -cycloalkyl, aryl, heteroaryl, heterocyclyl, -C₁₋₆aryl alkyl, -C₁₋₆heteroaryl alkyl, -C₁₋₆-heterocyclyl alkyl, -C₁₋₆C₍O₎ORᵃ alkyl, -C₂₋₆C₍O₎ORᵃ, -SO₂Rᵃ, -SO₂NRᵃRᵇ, -C (O) NRᵃSO₂Rᵃ, and C₁₋₆-C₃₋₈cycloalkyl alkyl; wherein each alkyl, alkenyl, cycloalkyl, aryl, heteroaryl or heterocyclyl is optionally substituted with 1 to 4 groups independently selected from -ORᵃ, -CN, halo, C₁₋₆ alkyl, -C₁₋₆ORᵃ alkyl, -C₁₋₆ alkyl-alkyl -haloalkyl C₁₋₆, cycloalkyl C₃₋₈, -alkyl C₁₋₃cycloalkyl C₃₋₈, -C (O) Rᵃ, -alkyl C₁₋₆C₍O₎Rᵃ, -C (O) ORᵃ, -C₁₋₆C₍ O₎ORᵃ, -NRᵃRᵇ, -OC (O) NRᵃRᵇ, NRᵃC (O) ORᵇ, -C₁₋₆NRᵃRᵇ alkyl, -C (O) NRᵃRᵇ, -C₁₋₆C₍O₎NRᵃRᵇ alkyl, -SO₂Rᵃ, -C₁₋ alkyl ₆SO₂Rᵃ, -SO₂NRᵃRᵇ, -CquSO₂NRᵃRᵇ alkyl, -C (O) NRᵃSO₂Rᵇ, -C₁₋₆C₍O₎NRᵃSO₂Rᵇ, -NRᵃC (O) Rᵇ, and -C₁₋₆NRᵃC (O) Rᵇ alkyl; each R² is independently selected from H, -C₁₋₆ alkyl, -C₂₋₆ alkenyl, -C₂₋₆ alkynyl, C₁₋₆ cycloalkyl, aryl, heteroaryl, heterocyclyl, -C₁₋₆aryl alkyl, -C₁₋₆heteroaryl alkyl, - C₁₋₆-heterocyclyl alkyl, -C₂₋₆-ORᵃ alkyl, -C₁₋₆C₍O₎ORᵃ alkyl, and -C₂₋₆C₍O₎ORᵃ alkyl; wherein each alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl or heterocyclyl is optionally substituted with 1 to 4 groups independently selected from -ORᵃ, -CN, halo, C₁₋₆ alkyl, -C₁₋₆ORᵃ alkyl, -C₁₋ alkyl-alkyl ₆, -haloalkyl C₁₋₆, -cycloalkyl C₃₋₈, -alkyl C₁₋₃cycloalkyl C₃₋₈, -C (O) Rᵃ, -alkyl C₁₋₆C₍O₎Rᵃ, -C (O) ORᵃ, -alkyl C₁ ₋₆C₍O₎ORᵃ, -NRᵃRᵇ, -C₁₋₆NRᵃRᵇ alkyl, -C (O) NRᵃRᵇ, C₁₋₆C₍O₎NRᵃRᵇ alkyl, -SO₂Rᵃ, -C₁₋₆SO₂Rᵃ alkyl, -SO₂NRᵃRᵇ, -C₁₋₆SO₂NRᵃRᵇ alkyl, -C (O) NRᵃSO₂Rᵇ and -NRᵃC (O) Rᵇ; or R¹ and R² combine to form a heterocyclyl group that optionally contains 1, 2 or 3 additional heteroatoms independently selected from oxygen, sulfur and nitrogen, and optionally substituted with 1 to 3 groups independently selected from oxo, -C₁₋₆ alkyl, - C₃₋₈ cycloalkyl, -C₂₋₆ -alkenyl, -C₂₋₆ -alkynyl, -ORᵃ, -C (O) ORᵃ, -cyanoalkyl-C₁₋₆, -alkyl-C₁₋₆ORᵃ, -haloalkyl-C₁₋₆, -alkyl-C₁₋₃ -cycloalkyl C₃₋₈, -C (O) Rᵃ, -C₁₋₆C₍O₎Rᵃ alkyl, -C₁₋₆C₍O₎ORᵃ alkyl, -NRᵃRᵇ, -C₁₋₆NRᵃRᵇ alkyl, -C (O) NRᵃRᵇ, -C₁ alkyl ₋₆C₍O₎NRᵃRᵇ, -SO₂Rᵃ, -C₁₋₆SO₂Rᵃ alkyl, -SO₂NRᵃRᵇ, and C₁₋₆SO₂NRᵃRᵇ alkyl; each R³ is independently H, -C₁₋₆ alkyl, -C₂₋₆ alkyl, -C₁₋₆ cycloalkyl, aryl, heteroaryl, heterocyclyl, -C₁₋₆aryl alkyl, -C₁₋₆-heteroaryl alkyl, -C₁₋₆-heterocyclyl alkyl, -alkyl C₂₋₆-ORᵃ, -C₁₋₆C₍O₎ORᵃ alkyl, or -C₂₋₆C₍O₎ORᵃ alkenyl; each R⁴ is independently H, -C₁₋₆ alkyl, -C₂₋₆ alkenyl, -C₃₋₆ cycloalkyl, aryl, heteroaryl, heterocyclyl, -C₁₋₆aryl alkyl, -C₁₋₆-heteroaryl alkyl, -C₁₋₆-heterocyclyl alkyl, -alkyl C₂₋₆-ORᵃ, C₁₋₆C₍O₎ORᵃ alkyl, or -C₂₋₆C₍O₎ORᵃ alkenyl; each Rᵃ is independently selected from H, -C₁₋₆ alkyl, -C₃₋₈ -cycloalkyl, aryl, heteroaryl, heterocyclyl, -C₁₋₃-C₃₋₈cycloalkyl, -C₁₋₆aryl alkyl, -C₁₋₆-heteroaryl alkyl, and -alkyl C₁₋₆heterocyclyl; each Rᵇ is independently selected from H, -C₁₋₆ alkyl, -C₃₋₈ -cycloalkyl, aryl, heteroaryl, heterocyclyl, -C₁₋₃-C₃₋₈cycloalkyl, -C₁₋₆aryl alkyl, -C₁₋₆-heteroaryl alkyl, and -alkyl C₁₋₆heterocyclyl; or Rᵃ and Rᵇ can be combined to form a ring consisting of 3-8 atoms in the ring that are C, N, O or S; wherein the ring is optionally substituted with 1 to 4 groups independently selected from -ORᶠ, -CN, halo, -C₁₋₆ORᶠ alkyl, -C₁₋₆ alkyl alkyl, -C₁₋₆ haloalkyl, C₃₋₈ cycloalkyl, -C₁ alkyl ₋₃C₃₋₈ cycloalkyl, -C (O) Rᶠ, -C₁₋₆C₍O₎Rᶠ alkyl, -C (O) ORᶠ, -C₁₋₆C₍O₎ORᶠ alkyl, -NRᶠRᵍ, -C₁₋₆NRᶠRᵍ alkyl, - C (O) NRᶠRᵍ, -C₁₋₆C₍O₎NRᶠRᵍ alkyl, -SO₂Rᶠ, -C₁₋₆SO₂Rᶠ alkyl, -SO₂NRᶠRᵍ, -C₁₋₆SO₂NRᶠRᵍ alkyl, -C (O) NRᶠSO₂Rᵍ and -NRᶠC (O) Rᵍ; each Rᶜ is independently selected from H, OH, -C₁₋₆ alkyl, -C₃₋₈ cycloalkyl, aryl, heteroaryl, heterocyclyl, -C₁₋₃-Ciclocycloalkyl, -C₁₋₆aryl alkyl, -C₁₋₆heteroaryl alkyl, and -C₁₋₆heterocyclyl alkyl; Rᵈ is independently selected from H, -C₁₋₆ -alkyl, -C₃₋₈ -cycloalkyl, aryl, heteroaryl, heterocyclyl, -C₃₋₈ -alkyl-C₃₋₈ -alkyl, -C₁₋₆aryl-alkyl, -C₁₋₆-heteroaryl-alkyl, and -C₁ -alkyl Teroheterocyclyl; each Rᵉ is independently selected from H, -C₁₋₆ alkyl, -O-C₁₋₆ alkyl, -C₃₋₈ cycloalkyl, aryl, heteroaryl, heterocyclyl, -O-C₃₋₈ cycloalkyl, -O-aryl, -O- heteroaryl, -O-heterocyclyl, -C₁₋₃-C₃₋₈cycloalkyl alkyl, -C₁₋₆aryl alkyl, -C₁₋₆heteroaryl alkyl, -NRᶠRᵍ, -C₁₋₆NRᶠRᵍ alkyl, -C (O) NRᶠRᵍ, -C₁₋₆C₍ alkyl O₎NRᶠRᵍ, -NHSO₂Rᶠ, -C₁₋₆SO₂Rᶠ alkyl, and -C₁₋₆SO₂NRᶠRᵍ alkyl; Rᶠ is independently selected from H, -C₁₋₆ alkyl, -C₃₋₈ cycloalkyl, aryl, heteroaryl, heterocyclyl, C₁₋₃-C alquilocycloalkyl alkyl, -C₁₋₆aryl alkyl, -C₁₋₆heteroaryl alkyl, and -C₁₋ alkyl Teroheterocyclyl; and Rᵍ is independently selected from H, -C₁₋₆ -alkyl, -C₃₋₈ -cycloalkyl, aryl, heteroaryl, heterocyclyl, -C₃₋₈ -alkyl-C₃₋₈ -alkyl, -C₁₋₆aryl-alkyl, -C₁₋₆-heteroaryl-alkyl, and -alkyl C₁₋₆heterocyclyl; or a pharmaceutically acceptable salt, stereoisomer, mixture of stereoisomers, solvate or tautomer thereof. |
| priorityDate | 2017-04-20^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
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