C07D487/02

Pyrrolopyrimidine compounds as inhibitors of protein kinases

The present invention relates to certain pyrrolopyrimidine derivatives, pharmaceutical compositions containing them, and methods of using them, including methods for the treatment of proliferation disorders and other diseases related to the dysregulation of kinase (such as, but not limited to, EGFR (including HER), Alk, PDGFR, BLK, BMX/ETK, BTK, FLT3(D835Y), ITK, JAK1, JAK2, JAK3, TEC and TXK) and/or the respective pathways.

QUINOXALINE AND PYRIDOPYRAZINE DERIVATIVES AS A PI3KB INHIBITORS

The present invention relates to substituted quinoxaline and pyridopyrazine derivatives of Formula (I)

##STR00001##

wherein the variables have the meaning defined in the claims. The compounds according to the present invention are useful as pI3K inhibitors. The invention further relates to pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.

LUMINOGENS FOR BIOLOGICAL APPLICATIONS
20200079787 · 2020-03-12 ·

A compound comprises a donor and an acceptor, wherein at least one donor (D) and at least one acceptor (A) may be arranged in an order of D-A; D-A-D; A-D-A; D-D-A-D-D; A-A-D-A-A; D-A-D-A-D; and A-D-A-D-A. The compound may be selected from the group consisting of: MTPE-TP, MTPE-TT, TPE-TPA-TT, PTZ-BT-TPA, NPB-TQ, TPE-TQ-A, MTPE-BTSe, DCDPP-2TPA, DCDPP-2TPA4M, DCDP-2TPA, DCDP-2TPA4M, TTS, ROpen-DTE-TPECM, and RClosed-DTE-TPECM. The compound may be used as a probe and may be functionalized with special targeted groups to image biological species. As non-limiting examples, the compound may be used in cellular cytoplasms or tissue imaging, blood vessel imaging, in vivo fluorescence imaging, brain vascular imaging, sentinel lymph node mapping, and tumor imaging, and the compound may be used as a photoacoustic agent.

LUMINOGENS FOR BIOLOGICAL APPLICATIONS
20200079787 · 2020-03-12 ·

A compound comprises a donor and an acceptor, wherein at least one donor (D) and at least one acceptor (A) may be arranged in an order of D-A; D-A-D; A-D-A; D-D-A-D-D; A-A-D-A-A; D-A-D-A-D; and A-D-A-D-A. The compound may be selected from the group consisting of: MTPE-TP, MTPE-TT, TPE-TPA-TT, PTZ-BT-TPA, NPB-TQ, TPE-TQ-A, MTPE-BTSe, DCDPP-2TPA, DCDPP-2TPA4M, DCDP-2TPA, DCDP-2TPA4M, TTS, ROpen-DTE-TPECM, and RClosed-DTE-TPECM. The compound may be used as a probe and may be functionalized with special targeted groups to image biological species. As non-limiting examples, the compound may be used in cellular cytoplasms or tissue imaging, blood vessel imaging, in vivo fluorescence imaging, brain vascular imaging, sentinel lymph node mapping, and tumor imaging, and the compound may be used as a photoacoustic agent.

Quinoxaline and pyridopyrazine derivatives as PI3Kβ inhibitors

The present invention relates to substituted quinoxaline and pyridopyrazine derivatives of Formula (I) ##STR00001##
wherein the variables have the meaning defined in the claims. The compounds according to the present invention are useful as pI3K inhibitors. The invention further relates to pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.

Quinoxaline and pyridopyrazine derivatives as PI3Kβ inhibitors

The present invention relates to substituted quinoxaline and pyridopyrazine derivatives of Formula (I) ##STR00001##
wherein the variables have the meaning defined in the claims. The compounds according to the present invention are useful as pI3K inhibitors. The invention further relates to pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.

Compound, display panel and display apparatus

Provided is a compound including a moiety A and one or two moieties B fused with the moiety A at fusing sites, in which X is N, O, S or C; and when X is O or S, Ar.sub.2-L.sub.1- is absent; Y.sub.1-Y.sub.4 are each independently C or N; L.sub.1 and L.sub.2 are each independently a single bond, a substituted or unsubstituted C6-C30 arylene, a substituted or unsubstituted C10-C40 fused arylene, or a substituted or unsubstituted C4-C30 heteroarylene; Ar.sub.1 and Ar.sub.2 are each independently a substituted or unsubstituted C6-C30 aryl, a substituted or unsubstituted C10-C40 fused aryl, a substituted or unsubstituted C4-C30 heteroaryl, or a substituted or unsubstituted C6-C40 fused heteroaryl, and * represents one of the fusing sites, N or CR.sub.a, where R.sub.a is a substituted or unsubstituted C1-C20 alkyl, a substituted or unsubstituted C6-C30 aryl, or a substituted or unsubstituted C3-C30 heteroaryl. ##STR00001##

Pyrazolo[1,5-a]pyrimidine-3-carboxamide derivatives useful in the treatment of psoriasis and systemic lupus erythematosus

The present invention provides a compound of Formula I: wherein R is methyl or ethyl; or a pharmaceutically acceptable salt thereof useful for treating psoriasis or systemic lupus erythematosus. ##STR00001##

Pyrazolo[1,5-a]pyrimidine-3-carboxamide derivatives useful in the treatment of psoriasis and systemic lupus erythematosus

The present invention provides a compound of Formula I: wherein R is methyl or ethyl; or a pharmaceutically acceptable salt thereof useful for treating psoriasis or systemic lupus erythematosus. ##STR00001##

PREPARATION AND APPLICATION METHOD OF HETEROCYCLIC COMPOUNDS AS KRAS INHIBITOR

Disclosed is a compound of formula (I) or a pharmaceutically acceptable salt, prodrug, tautomer or stereoisomer, and solvate thereof. The compound can be applied to treatment of cancers and inflammations of mammals. Further disclosed are a preparation method for the compound of formula (I) and a pharmaceutical composition containing the compound.

##STR00001##