http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-090548-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_a73cee5001ad08339ae751c10d9abf71 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P17-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C53-18 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P29-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P19-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P37-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D487-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-519 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-553 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-519 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P17-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P37-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P19-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D487-04 |
| filingDate | 2013-03-27-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2014-11-19-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-090548-A1 |
| titleOfInvention | BICYCLIC AZAHETEROCICLOBENCILAMINS AS PI3K INHIBITORS |
| abstract | They modulate the activity of phosphoinositide 3-kinases (PI3K) and are useful in the treatment of diseases related to the activity of PI3K, which includes, for example, inflammatory disorders, immune-based disorders, cancer and other diseases. Claim 1: A compound of formula (1) or a pharmaceutically acceptable salt thereof, wherein: V is C (= O), S (= O) ₂, CH₂, CHR³ᶜ, and CR³ᶜR³ᶜ; T is C (= O), S (= O) ₂, CH₂, CHR³ᵃ, and CR³ᵃR³ᵃ; Q is C (= O), S (= O) ₂, (CH₂) ₙ, (CHR³ᵃ) ₙ, and (CR³ᵃR³ᵃ) ₙ; where n is 0, 1, or 2; U is O or NR³ᵈ; provided that when T is C (= O) or S (= O) ₂, Q is (CH₂) ₙ, (CHR³ᵃ) ₙ, or - (CR³ᵃR³ᵃ) ₙ; and provided that when Q is C (= O) or S (= O) ₂, T is CH₂, CHR³ᵃ, or CR³ᵃR³ᵃ and U is NR³ᵈ; RA is H or C₁₋₃ alkyl; Ar is a residue of formula (2), (3), (4) or (5); X¹ is CH or N; Y¹ is CH or N; or alternatively, RA and Ar, together with the N to which they are attached, combine to form a functional group of formula (6); X is CR⁹ or N; W is CR⁷ or N; Y is CR⁸, CR⁸ᵃ, or N; Z is a bond or C (= O); provided that -W = YZ- is -CR⁷ = CR⁸-, -N = CR⁸-, -CR⁷ = CR⁸ᵃ-C (= O) -, -N = CR⁸ᵃ-C (= O) -, or -CR⁷ = NC ( = O) -; R¹ is C₁₋₃ alkyl; each R³ᵃ is independently selected from C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₁₋₆ haloalkyl, and Cy¹; wherein said C₁₋₆ alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynyl are each optionally substituted with 1, 2, or 3 independently selected R¹¹ groups; R³ᵇ is H, Cy, - (C₁₋₃ alkylene) -Cy, C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₁₋₆ haloalkyl, C₍₌O₎Rᵇ, C (= O) NRᶜRᵈ, C (= O) ORᵃ, C (= NRᵉ) Rᵇ, C (= NRᵉ) NRᶜRᵈ, S (= O) ₂Rᵇ, or S (= O) ₂NRᶜRᵈ; wherein said C₁₋₆ alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynyl are each optionally substituted by 1, 2, 3, or 4 independently selected R¹³ᵇ groups; each R³ᶜ is independently selected from C₁₋₄ alkyl, C₁₋₄ haloalkyl, C₁₋₄ alkoxy-C₁₋₄ alkyl, and C₁₋₄ haloalkoxy-C alquilo alkyl; R³ᵈ is H, C₁₋₄ alkyl, C₁₋₄ haloalkyl, C₁₋₄ alkoxy-C₁₋₄ alkyl, or C₁₋₄ haloalkoxy-C alquilo alkyl; R⁴ is H, halo, OH, CN, C₁₋₄ alkyl, C₁₋₄ haloalkyl, C₁₋₄ alkoxy, or C₁₋₄ haloalkoxy; R⁵ is halo, OH, CN, C₁₋₄ alkyl, C₁₋₄ haloalkyl, C₁₋₄ alkoxy, C₁₋₄ haloalkoxy, or cyclopropyl; R⁶ is H, halo, OH, CN, C₁₋₄ alkyl, C₁₋₄ haloalkyl, C₁₋₄ alkoxy, or C₁₋₄ haloalkoxy; R⁷ is H or C₁₋₄ alkyl; R⁸ is H, halo, -OH, -CN, C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₁₋₆ haloalkyl, Cy², - (C₁₋₃ alkylene) -Cy², ORᵃ², SRᵃ², C ( = O) Rᵇ², C (= O) NRᶜ²Rᵈ², C (= O) ORᵃ², OC (= O) Rᵇ², OC (= O) NRᶜ²Rᵈ², NRᶜ²Rᵈ², NRᶜ²C (= O) Rᵇ², NRᶜ²C (= O) ORᵇ², NRᶜ²C (= O) NRᶜ²Rᵈ², C (= NRᵉ) Rᵇ², C (= NRᵉ) NRᶜ²Rᵈ², NRᶜ²C (= NRᵉ) NRᶜ²Rᵈ², NRᶜ²S (= O) Rᵇ², NRᶜ²S (= O) ₂NRᶜ²Rᵈ², S (= O) Rᵇ², S ( = O) ₂Rᵇ², or S (= O) ₂NRᶜ²Rᵈ²; wherein said C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl is each optionally substituted by 1, 2, 3, or 4 independently selected R¹¹ groups; R⁸ᵃ is H, halo, -CN, C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₁₋₆ haloalkyl, Cy², - (C₁₋₃ alkylene) -Cy², C (= O) Rᵇ², C ( = O) NRᶜ²Rᵈ², C (= O) ORᵃ², NRᶜ²Rᵈ², NRᶜ²C (= O) Rᵇ², NRᶜ²C (= O) ORᵇ², NRᶜ²C (= O) NRᶜ²Rᵈ², NRᶜ²S (= O) Rᵇ², NRᶜ²S (= O) ₂NRᶜ²Rᵈ², S (= O) Rᵇ², S (= O) ₂Rᵇ², or S (= O) ₂NRᶜ²Rᵈ²; wherein said C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl is each optionally substituted by 1, 2, 3, or 4 independently selected R¹¹ groups; R⁹ is H, halo, OH, CN, C₁₋₄ alkyl, C₁₋₄ haloalkyl, C₁₋₄ alkoxy, or C₁₋₄ haloalkoxy; R¹⁰ is H or C₁₋₄ alkyl; each R¹¹ is independently selected from halo, OH, NO₂, CN, C₁₋₃- alkyl, C₂₋₃ alkenyl, C₂₋₃ alkynyl, C₁₋₃ haloalkyl, Ciano cyano-alkyl, HO-C₁₋₃ alkyl, alkoxy C₁₋₃-C₁₋₃ alkyl, C₃₋₇ cycloalkyl, C₁₋₃ alkoxy, C₁₋₃ haloalkoxy, amino, C₁₋₃amino alkyl, di (C₁₋₃ alkyl) amino, thio, C₁₋₃thio alkyl, C₁₋ alkyl Finsulfinil, C₁₋₃sulfonyl alkyl, carbamyl, C₁₋₃carbamyl alkyl, di (C₁₋₃ alkyl) carbamyl, carboxy, C₁₋₃carbonyl alkyl, C₁₋₄carbonyl alkoxy, C₁₋₃carbonylamino, C₁₋₃sulfonylamino alkyl, aminosulfonyl, C₁₋ alkyl Inosaminosulfonyl, di (C₁₋₃ alkyl) aminosulfonyl, aminosulfonylamino, C₁₋₃aminosulfonylamino alkyl, di (C₁₋₃ alkyl) aminosulfonylamino, aminocarbonylamino, C₁₋₃aminocarbonylamino, and di (C₁₋₃ alkyl) aminocarbonylamino; each R¹³ᵇ is independently selected from Cy¹, - (C₁₋₃ alkylene) -Cy¹, halo, CN, NO₂, C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₁₋₆ haloalkyl, ORᵃ¹, SRᵃ¹, C ( = O) Rᵇ¹, C (= O) NRᶜ¹Rᵈ¹, C (= O) ORᵃ¹, OC (= O) Rᵇ¹, OC (= O) NRᶜ¹Rᵈ¹, NRᶜ¹Rᵈ¹, NRᶜ¹C (= O) Rᵇ¹, NRᶜ¹C (= O) ORᵇ¹, NRᶜ¹C (= O) NRᶜ¹Rᵈ¹, C (= NRᵉ) Rᵇ¹, C (= NRᵉ) NRᶜ¹Rᵈ¹, NRᶜ¹C (= NRᵉ) NRᶜ¹Rᵈ¹, NRᶜ¹S (= O) Rᵇ¹, NRᶜ¹S (= O) ₂NRᶜ¹Rᵈ¹, S (= O) Rᵇ¹, S ( = O) ₂Rᵇ¹, S (= O) ₂NRᶜ¹Rᵈ¹; wherein said C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl is each optionally substituted with 1, 2, or 3 independently selected R¹¹ groups; each Cy is independently selected from C₃₋₇ cycloalkyl, 4-10 membered heterocycloalkyl, phenyl, naphthyl and 5-10 membered heteroaryl, wherein said C₃₋₇ cycloalkyl, 4-10 membered heterocycloalkyl, phenyl, naphthyl and heteroaryl of 5 - 10 members are optionally substituted with 1, 2, 3, or 4 independently selected R¹³ᵇ groups; each Rᵃ, Rᶜ, and Rᵈ is independently selected from H, C₁₋₆ alkyl, C₁₋₆ haloalkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, and Cy; wherein said C₁₋₆ alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynyl are each optionally substituted with 1, 2, or 3 independently selected R¹³ᵇ groups; each Rᵇ is independently selected from C₁₋₆ alkyl, C₁₋₆ haloalkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, and Cy; wherein said C₁₋₆ alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynyl are each optionally substituted with 1, 2, or 3 independently selected R¹³ᵇ groups; or alternatively, Rᶜ and Rᵈ together with the N atom to which they are attached form a 4-, 5-, 6- or 7- membered heterocycloalkyl group, which is optionally substituted with 1, 2, or 3 independently selected R¹³ᵇ groups; each Rᵉ is independently selected from H, CN, OH, C₁₋₄ alkyl, and C₁₋₄ alkoxy; each Cy¹ is independently selected from C₃₋₇ cycloalkyl, 4-7 membered heterocycloalkyl, 5-6 membered phenyl and heteroaryl, wherein said C₃₋₇ cycloalkyl, 4-7 membered heterocycloalkyl, 5-6 membered phenyl and heteroaryl are option |
| priorityDate | 2012-04-02-04:00^^<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: 30.