http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-120846-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_dcce39a20bef16c3f04497659caba40f http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_3fef52dfd583ecdd45acd228f75bd26e |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4545 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-454 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D471-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4525 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D417-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D417-12 |
| filingDate | 2020-12-21-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_8c3d21f5367ca70f796acf0b3cdd3091 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_fb58520d34ae26d73dff5729cefa9765 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_b0c7cbd98e065f7850b17d578a074b28 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_9f38fcc83a27d1b2c9e269e8204574f2 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_61a053f162f9efc44cf2dc30ad606384 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_907a16699ad372b1a99acb77782c922e http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_302ae750b348ba3e8601266fdec9e8a2 |
| publicationDate | 2022-03-23-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-120846-A1 |
| titleOfInvention | PROTEIN TYROSINE PHOSPHATASE DEGRADATORS AND METHODS OF USE OF SUCH |
| abstract | Provided herein are compounds, compositions, and methods useful for degrading protein tyrosine phosphatase, e.g. protein tyrosine phosphatase non-receptor type 2 (PTPN2) and/or protein tyrosine phosphatase non-receptor type 1 (PTPN1), and to treat related diseases that respond favorably to treatment with PTPN1 or PTPN2 inhibitors, e.g. eg, cancer or metabolic disease. Claim 1: A compound of formula (1) or a pharmaceutically acceptable salt thereof, wherein: R¹ is hydrogen or halogen; R² is hydrogen, halogen, C₁₋₃ alkoxy, C₃₋₆ cycloalkoxy, C₁₋₃ haloalkoxy, C₃₋₅ halocycloalkoxy, C₁₋₃ alkyl, C₁₋₃ haloalkyl, C₃₋₆ cycloalkyl, or -L-Z; R³ is hydrogen, halogen, C₁₋₃ alkoxy, C₃₋₅ cycloalkoxy, C₁₋₃ haloalkoxy, C₃₋₅ halocycloalkoxy, C₁₋₃ alkyl, C₁₋₃ haloalkyl, C₃₋₅ cycloalkyl, or -L-Z; wherein one of R² and R³ is -L-Z and the other of R² and R³ is not -L-Z; Rˣ is hydrogen or halogen; L is -U-V-W-X-Y-; U is a bond, -(NR⁴)-, -O-, C₁₋₃ alkylene, C₂₋₃ alkenylene, C₂₋₃ alkynylene, C₃₋₆ cycloalkylene, 4-10 membered heterocyclylene, 5-10 membered heteroarylene, - (C=O)NR⁴-, -NR⁴(C=O)-, -OR⁵-, -R⁵O-, -NR⁴R⁵-, -R⁵NR⁴-, or -(NR⁴)(C=O)(NR⁴)-; each R⁴ is independently a hydrogen, C₁₋₆ alkyl or C₃₋₅ cycloalkyl; R⁵ is C₁₋₃ alkylene, C₃₋₇ cycloalkylene, or 4-12 membered heterocyclylene; V is a bond, -(NR⁴)-, -O-, C₁₋₆ alkylene, C₂₋₆ alkenylene, -(C=O)NR⁴-, -(NR⁴)R⁵-, -(NR⁴)(C=O) -, -NH(C=O)NH-, -OR⁵-, -R⁵O-, 4-10 membered heterocyclylene, 5-10 membered heteroarylene, C₆₋₁₀ arylene, or C₃₋₆ cycloalkylene; W is a bond, C₁₋₃ alkylene optionally substituted with hydroxyl, C₃₋₆ cycloalkylene, 4-12 membered heterocyclylene, -O-, -(NR⁴)-, -R⁵(NR⁴)-, -(NR⁴)R⁵-, -(NR⁴)(C=O)-, -R⁵(NR⁴)(C=O)-, -(C=O)(NR⁴)R⁵-, -R⁵(C=O)(NR⁴)-, -(C =O)(NR⁴)-, -R⁵(C=O)-, -(C=O)R⁵-, -(C=O)-, -(S=O)-, or -S(O₂)-; X is a bond, C₁₋₃ alkylene, C₃₋₆ cycloalkylene, 4-12 membered heterocyclylene, C₆₋₁₀ arylene, 5-10 membered heteroarylene, -R⁵(NR⁴)(C=O)-, -(C= O)R⁵(NR⁴)-, -R⁵(C=O)(NR⁴)-, -(NR⁴)(C=O)R⁵-, -R⁵(C=O)(NR⁴)-, -(C=O) (NR⁴)R⁵-, -(NR⁴)R⁵(C=O)-, -R⁵(C=O)(NR⁴)R⁵-, -R⁵(NR⁴)(C=O)R⁵-, -(C=O) R⁵-, or -R⁵(C=O)-; Y is R⁶, R⁶(CRARB)ₚ-Q-, or -Q-(CRARB)ₚR⁶-; Q is -(NR⁴)-, -O- or -(CRARB)ₚ-; p is 0, 1, 2 or 3; R⁶ is C₁₋₃ alkylene, C₃₋₇ cycloalkylene, 4-12 membered heterocyclylene, C₆₋₁₀ arylene, or 5-10 membered heteroarylene; wherein the heterocyclylene, heteroarylene, arylene and cycloalkylene groups of U, V, W, X and R⁶ are each optionally substituted with 1-3 substituents independently selected from fluoro, hydroxyl, C₁₋₆ alkoxy and C₁₋₆ alkyl; each RA and RB is independently hydrogen, fluoro, or C₁₋₆ alkyl; or RA and RB, together with the carbon atom to which they are attached, come together to form a C₃₋₄ cycloalkyl; or RA and RB combine to form oxo; Z is selected from the group consisting of the compounds of the group of formulas (2); R⁷ is hydrogen, C₁₋₆ alkyl optionally substituted with a group selected from hydroxy, cyano, and C₁₋₆ alkoxy, C₁₋₆ haloalkyl, C₃₋₆ cycloalkyl, 4-6 membered heterocyclyl, -(CRARB)(4-heterocyclyl). 12-membered), or -(CRARB)(C₃₋₆cycloalkyl); R⁸ is hydrogen or C₁₋₆ alkyl; each R⁹ is hydrogen, halogen, cyano, C₁₋₆ alkyl, C₁₋₆ haloalkyl, C₁₋₆ alkoxy, C₁₋₅ cycloalkoxy, 5-10 membered heteroaryloxy, or phenoxy; q is 0, 1 or 2; and each R¹⁰ is independently hydrogen, halogen, cyano, C₁₋₆ alkyl, C₃₋₆ cycloalkyl, or C₁₋₆ haloalkyl. |
| priorityDate | 2019-12-20-04:00^^<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: 39.