http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-115946-A1

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Predicate Object
assignee http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_d21cbff64022f95c237c0bd3ec8656ca
classificationIPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P35-00
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-04
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-438
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http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D491-10
filingDate 2019-08-09-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_c3906623935cf7147be485577e9b6257
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_cfc1eb31fba08c208a1916a5ff14351b
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http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_2dc4c675bc593f160375e1383d1db0fb
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_ff3982fd1c6ef7e9b844a23a3e1158bd
publicationDate 2021-03-17-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber AR-115946-A1
titleOfInvention PTPN11 INHIBITORS
abstract Claim 1: A compound represented by formula (1) or a salt, ester, or prodrug thereof, characterized in that: the subscript a is 0 or 1; the subscript b is 0 or 1; Y¹ is a direct link or CR¹⁷R¹⁸; Y² is selected from the group consisting of C₁₋₄alkyl, amino, C₁₋₄alkylC (O) O-, C₁₋₄alkylamino, and C₁₋₄aminoalkyl; R¹ is selected from the group consisting of C₆₋₁₀aryl, C₃₋₈cycloalkyl, C₃₋₈cycloalkenyl, and a 5-10 membered heteroaryl group having 1 to 4 heteroatoms or groups as ring vertices independently selected from N, C (O ), O, and S; said aryl or heteroaryl of R¹ is optionally substituted with 1 to 5 R¹² groups independently selected from the group consisting of halo, hydroxy, amino, C₁₋₄alkylamino, di (C₁₋₄alkyl) amino, cyano, C₁₋₄alkyl, C₁₋₄alkoxy , C₁₋₄hydroxyalkyl, C₁₋₄haloalkyl, C₁₋₄aminoalkyl, C₃₋₈cycloalkyl, C₃₋₈cycloalkenyl, NR¹⁵C (O) R¹⁴, NR¹⁵C (O) OR¹⁴, NR¹⁴C (O) NR¹⁵R¹⁶, NR¹⁵S (O) R¹⁴, NR¹⁵S (O) ₂R¹⁴ , C (O) NR¹⁵R¹⁶, S (O) NR¹⁵R¹⁶, S (O) ₂NR¹⁵R¹⁶, C (O) R¹⁴, C (O) OR¹⁴, OR¹⁴, SR¹⁴, S (O) R¹⁴, and S (O) ₂R¹⁴; R², R³, R¹⁰, and R¹¹ are each independently selected from the group consisting of hydrogen, C₁₋₄alkyl, and Cycloalkyl; R⁴, R⁵, R⁸, and R⁹ are each independently selected from the group consisting of hydrogen, C₁₋₄alkyl, C₁₋₄alkoxy, amino, hydroxy, C₃-cycloalkyl, halo, and C₁₋₄alkylamino; R⁶ is selected from the group consisting of amino, C₁₋₄-aminoalkyl, and C₁₋₄alkylamino; R⁷ is selected from the group consisting of hydrogen, amido, cyano, halo, and hydroxy, or is selected from the group consisting of C₁₋₄alkyl, C₁₋₄hydroxyalkyl, C₃₋₆cycloalkyl, phenyl, and 5- or 6-membered heteroaryl , any of which is optionally substituted with one to five groups independently selected from the group consisting of amino, halo, hydroxy, cyano, C₁₋₄alkyl, C₁₋₄alkoxy, C₁₋₄haloalkyl, C₁₋₄haloalkoxy, C₁₋₄alkylamino, and C₁₋₄aminoalkyl; or R⁶ and R⁷ together with the carbon atom to which they are both attached form a 3- to 7-membered saturated or unsaturated ring, having 0 to 3 heteroatoms or groups as vertices of the ring independently selected from N, C (O), O , and S (O) ₘ; the subscript m is 0, 1, or 2; said saturated or unsaturated ring formed by R⁶ and R⁷ is unsubstituted or is substituted with 1 to 3 groups independently selected from the group consisting of amino, halo, hydroxy, cyano, C₁₋₄alkyl, C₁₋₄alkoxy, C₁₋₄haloalkyl, C₁ ₋₄haloalkoxy, C₁₋₄alkylamino and C₁₋₄aminoalkyl; Any two groups of R², R³, R⁴, R⁵, R⁷, R⁸, R⁹, R¹⁰ and R¹¹ can form a 5 to 6 membered ring, having 0 to 2 heteroatoms as ring vertices selected from N, O and S; Any two groups of R², R⁴, R⁶, R⁸ and R¹⁰ can form a direct bond, or a carbon bridge of 1 or 2 atoms; R¹³ is selected from the group consisting of hydrogen, halo, cyano, C₁₋₆alkyl, C₁₋₆haloalkyl, C₁₋₆hydroxyalkyl, C₁₋₆dihydroxyalkyl, -NH-NHR¹⁹, -NHR¹⁹, -OR¹⁹, -NHC (O) R¹⁹, - NHC (O) NHR¹⁹, -NHS (O) ₂NHR¹⁹, -NHS (O) ₂R¹⁹, -C (O) OR¹⁹, -C (O) NR¹⁹R²⁰, -C (O) NH (CH₂) qOH, -C (O) NH (CH₂) qR²¹, -C (O) R²¹, -NH₂, -OH, -S (O) ₂NR¹⁹R²⁰, C₃₋₈cycloalkyl, aryl, heterocyclyl having 1 - 5 heteroatoms as ring vertices selected from N, O, S and P, heteroaryl having 1-5 heteroatoms as ring vertices selected from N, O, S and P; where the subscript q is an integer from 0 to 6; and wherein aryl, heteroaryl, heterocyclyl, and cycloalkyl are substituted with 0 to 3 groups independently selected from the group consisting of C₁₋₄alkyl, -OH, -NH₂, -OR²¹, halo, cyano, and oxo; R¹⁴, R¹⁵, and R¹⁶ are each independently selected from the group consisting of hydrogen, C₁₋₄alkyl, C₃₋₈cycloalkyl, C₆₋₁₀aryl, and 5-10 membered heteroaryl, each of which is optionally substituted by one or further groups independently selected from the group consisting of amido, amino, halo, hydroxy, cyano, C₁₋₄alkyl, C₁₋₄alkoxy, C₁₋₄haloalkyl, C₁₋₄haloalkoxy, C₁₋₄alkylamino, and C₁₋₄aminoalkyl; R¹⁷ and R¹⁸ are each independently selected from the group consisting of hydrogen, C₁₋₄alkyl, and CF₃; R¹⁹ and R²⁰ are each independently selected from the group consisting of hydrogen, C₁₋₆alkyl, C₁₋₆haloalkyl, C₁₋₆hydroxyalkyl, C₂₋₆alkenyl, C₂₋₆alkynyl, and C₃₋₆cycloalkyl; and each R²¹ is independently selected from the group consisting of hydrogen, -OH, C₁₋₆alkyl, C₁₋₆haloalkyl, C₁₋₆alkylalkyl, C₂₋₆alkenyl, C₂₋₆alkynyl, and C₃₋₆cycloalkyl.
priorityDate 2018-08-10-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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