2,5-DISUBSTITUTED 3-METHYL PYRAZINES AND 2,5,6-TRISUBSTITUTED 3-METHYL PYRAZINES AS ALLOSTERIC SHP2 INHIBITORS

• Main Authors: ANDREAS BUCKL, ASHUTOSH JOGALEKAR, ELENA S KOLTUN, KEVIN MELLEM, NAING AAY, CHRISTOPHER SEMKO, GERT KISS, WALTER WON, ADRIAN GILL
• Format: Patent
• Language: English; Japanese
• Published: 11.11.2021
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

To provide: inhibitors of SH2 domain-containing protein tyrosine phosphatase-2 (SHP2); and their use in treatment of disease.SOLUTION: This invention relates to compounds expressed by the following general formula, or pharmaceutically acceptable salts, prodrugs, solvates, hydrates, tautomers, or isomers thereof. In the formula, A is a 5- to 12-membered monocyclic or polycyclic cycloalkyl, heterocycloalkyl, aryl, or heteroaryl; Y1 is -S-, a direct bond or the like; and Y2 is - NH-, -(CH2)m-, -C(O)-, -CH2NH- or the like.SELECTED DRAWING: None 【課題】ＳＨ２ドメイン含有タンパク質チロシンホスファターゼ−２（ＳＨＰ２）の阻害剤および疾患の処置におけるそれらの使用を提供する。【解決手段】下記一般式で表される化合物、またはその薬学的に許容される塩、プロドラッグ、溶媒和物、水和物、互変異性体および異性体による。式中、Ａは、５員から１２員の単環式または多環式のシクロアルキル、ヘテロシクロアルキル、アリールまたはヘテロアリール；Ｙ１は、−Ｓ−または直接結合等；Ｙ２は、−ＮＨ−、−（ＣＨ２）ｍ−、−Ｃ（Ｏ）−、−ＣＨ２ＮＨ−等を表す。【選択図】なし