C07D487/02

LUMINOGENS FOR BIOLOGICAL APPLICATIONS
20220048923 · 2022-02-17 ·

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-TP A-TT, PTZ-BT-TP A, NPB-TQ, TPE-TQ-A, MTPE-BTSe, DCDPP-2TP A, 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
20220048923 · 2022-02-17 ·

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-TP A-TT, PTZ-BT-TP A, NPB-TQ, TPE-TQ-A, MTPE-BTSe, DCDPP-2TP A, 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.

NOVEL PYRROLOPYRIMIDINE COMPOUNDS AS INHIBITORS OF PROTEIN KINASES
20170224689 · 2017-08-10 · ·

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.

PESTICIDALLY ACTIVE HETEROCYCLIC DERIVATIVES WITH SULPHUR CONTAINING SUBSTITUENTS

Compounds of formula (I), wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts salts, stereoisomers, enantiomers, tautomers and N-oxides of those compounds, can be used as insecticides and can be prepared in a manner known per se.

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PESTICIDALLY ACTIVE HETEROCYCLIC DERIVATIVES WITH SULPHUR CONTAINING SUBSTITUENTS

Compounds of formula (I), wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts salts, stereoisomers, enantiomers, tautomers and N-oxides of those compounds, can be used as insecticides and can be prepared in a manner known per se.

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3-(PHENYLSULFONYL)-[1,2,3]TRIAZOLO[1,5A]QUINAZOLIN-5(4H)-ONE DERIVATIVES

The present invention relates to a compound according to formula (I), wherein R1 and R5 are independently selected from H, halogen, hydroxyl, NO.sub.2, CN, C.sub.1-C.sub.6-alkyl optionally substituted by one or more R11, C.sub.1-C.sub.6-alkoxy optionally substituted by one or more R11, C.sub.3-C.sub.6-cycloalkyl optionally substituted by one or more R11, —C.sub.n-alkyl-N(R12)(R13) with n=0-3, —C.sub.n-alkyl-C(O)N(R12)(R13) with n=0-3, —SO.sub.2—N(R14)-C(O)—R15; —C.sub.n-alkyl-N(R14)-C(O)—R15 with n=0-3, —C.sub.n-alkyl-C(O)—OR16 with n=0-3, —O(C.sub.1-C.sub.3-alkyl-O).sub.m—C.sub.1-C.sub.3-alkyl-OR10 with m=0-3, —C.sub.n-alkyl-OR16 with n=0-3, —NH—C.sub.n-alkyl-R18 with n=0-3; —O—C.sub.n-alkyl-R18 with n=0-3; —OPO(OR10).sub.2, —PO(OR10).sub.2, and a heterocycle optionally substituted by one or more R17; R3 is selected from halogen, hydroxyl, NO.sub.2, CN, C.sub.1-C.sub.6-alkyl optionally substituted by one or more R11, C.sub.1-C.sub.6-alkoxy optionally substituted by one or more R11, C.sub.3-C.sub.6-cycloalkyl optionally substituted by one or more R11, —C.sub.n-alkyl-N(R12)(R13) with n=0-3, —C.sub.n-alkyl-C(O)N(R12)(R13) with n=0-3, —SO.sub.2—N(R14)-C(O)—R15; —C.sub.n-alkyl-N(R14)-C(O)—R15 with n=0-3, —C.sub.n-alkyl-C(O)—OR16 with n=0-3, —O(C.sub.1-C.sub.3-alkyl-O).sub.m—C.sub.1-C.sub.3-alkyl-OR10 with m=0-3, —C.sub.n-alkyl-OR16 with n=0-3, —NH—C.sub.n-alkyl-R18 with n=0-3; —O—C.sub.n-alkyl-R18 with n=0-3; —OPO(OR10).sub.2, —PO(OR10).sub.2, and a heterocycle optionally substituted by one or more R17; R2 and R4 are independently selected from H, halogen, C.sub.1-C.sub.6-alkyl optionally substituted by one or more R11; R6, R7, R8 and R9 are independently selected from H, halogen, hydroxyl, NO.sub.2, CN, C.sub.1-C.sub.6-alkyl optionally substituted by one or more R11, C.sub.1-C6-alkoxy optionally substituted by one or more R11, C.sub.3-C.sub.6-cycloalkyl optionally substituted by one or more R11, —C.sub.n-alkyl-N(R12)(R13) with n=0-3, —C.sub.n-alkyl-C(O)N(R12)(R13) with n=0-3, —SO.sub.2—N(R12) (R13), —SO.sub.2—N(R14)-C(O)—R15; —C.sub.n-alkyl-N(R14)-C(O)—R15 with n=0-3, —C.sub.n-alkyl-C(O)—OR16 with n=0-3, —O(C.sub.1-C.sub.3-alkyl-O).sub.m—C.sub.1-C.sub.3-alkyl-OR10 with m=0-3, —C.sub.n-alkyl-OR16 with n=0-3, —NH—C.sub.n-alkyl-R18 with n=0-3; —O—C.sub.n-alkyl-R18 with n=0-3; —OPO(OR10).sub.2, —PO(OR10).sub.2, and a heterocycle optionally substituted by one or more R17; R10 is selected from H and C.sub.1-C.sub.6-alkyl optionally substituted by one or more R11; said one or more R11 is independently selected from Cl, F and hydroxy; R12, R13, R14, R15 and

3-(PHENYLSULFONYL)-[1,2,3]TRIAZOLO[1,5A]QUINAZOLIN-5(4H)-ONE DERIVATIVES

The present invention relates to a compound according to formula (I), wherein R1 and R5 are independently selected from H, halogen, hydroxyl, NO.sub.2, CN, C.sub.1-C.sub.6-alkyl optionally substituted by one or more R11, C.sub.1-C.sub.6-alkoxy optionally substituted by one or more R11, C.sub.3-C.sub.6-cycloalkyl optionally substituted by one or more R11, —C.sub.n-alkyl-N(R12)(R13) with n=0-3, —C.sub.n-alkyl-C(O)N(R12)(R13) with n=0-3, —SO.sub.2—N(R14)-C(O)—R15; —C.sub.n-alkyl-N(R14)-C(O)—R15 with n=0-3, —C.sub.n-alkyl-C(O)—OR16 with n=0-3, —O(C.sub.1-C.sub.3-alkyl-O).sub.m—C.sub.1-C.sub.3-alkyl-OR10 with m=0-3, —C.sub.n-alkyl-OR16 with n=0-3, —NH—C.sub.n-alkyl-R18 with n=0-3; —O—C.sub.n-alkyl-R18 with n=0-3; —OPO(OR10).sub.2, —PO(OR10).sub.2, and a heterocycle optionally substituted by one or more R17; R3 is selected from halogen, hydroxyl, NO.sub.2, CN, C.sub.1-C.sub.6-alkyl optionally substituted by one or more R11, C.sub.1-C.sub.6-alkoxy optionally substituted by one or more R11, C.sub.3-C.sub.6-cycloalkyl optionally substituted by one or more R11, —C.sub.n-alkyl-N(R12)(R13) with n=0-3, —C.sub.n-alkyl-C(O)N(R12)(R13) with n=0-3, —SO.sub.2—N(R14)-C(O)—R15; —C.sub.n-alkyl-N(R14)-C(O)—R15 with n=0-3, —C.sub.n-alkyl-C(O)—OR16 with n=0-3, —O(C.sub.1-C.sub.3-alkyl-O).sub.m—C.sub.1-C.sub.3-alkyl-OR10 with m=0-3, —C.sub.n-alkyl-OR16 with n=0-3, —NH—C.sub.n-alkyl-R18 with n=0-3; —O—C.sub.n-alkyl-R18 with n=0-3; —OPO(OR10).sub.2, —PO(OR10).sub.2, and a heterocycle optionally substituted by one or more R17; R2 and R4 are independently selected from H, halogen, C.sub.1-C.sub.6-alkyl optionally substituted by one or more R11; R6, R7, R8 and R9 are independently selected from H, halogen, hydroxyl, NO.sub.2, CN, C.sub.1-C.sub.6-alkyl optionally substituted by one or more R11, C.sub.1-C6-alkoxy optionally substituted by one or more R11, C.sub.3-C.sub.6-cycloalkyl optionally substituted by one or more R11, —C.sub.n-alkyl-N(R12)(R13) with n=0-3, —C.sub.n-alkyl-C(O)N(R12)(R13) with n=0-3, —SO.sub.2—N(R12) (R13), —SO.sub.2—N(R14)-C(O)—R15; —C.sub.n-alkyl-N(R14)-C(O)—R15 with n=0-3, —C.sub.n-alkyl-C(O)—OR16 with n=0-3, —O(C.sub.1-C.sub.3-alkyl-O).sub.m—C.sub.1-C.sub.3-alkyl-OR10 with m=0-3, —C.sub.n-alkyl-OR16 with n=0-3, —NH—C.sub.n-alkyl-R18 with n=0-3; —O—C.sub.n-alkyl-R18 with n=0-3; —OPO(OR10).sub.2, —PO(OR10).sub.2, and a heterocycle optionally substituted by one or more R17; R10 is selected from H and C.sub.1-C.sub.6-alkyl optionally substituted by one or more R11; said one or more R11 is independently selected from Cl, F and hydroxy; R12, R13, R14, R15 and

Luminogens for biological applications

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

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.

PYRAZOLOPYRIMIDINE COMPOUNDS AND USES THEREOF

Disclosed are compounds of Formula (I), methods of using the compounds for inhibiting ALK2 activity and/or FGFR activity, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders associated with ALK2 activity and/or FGFR activity, such as cancer.

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