C07D285/14

SOX11 INHIBITORS FOR TREATING MANTLE CELL LYMPHOMA

Disclosed are compounds that are chemical inhibitors of SOX11. The compounds disclosed are useful in treatment of various cancers.

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.

ACTIVATOR OF TREK (TWIK RELATED K+ CHANNELS) CHANNELS

Disclosed is a compound of formula (I):

##STR00001## wherein all symbols are defined in the description. Also disclosed are pharmaceutical compositions comprising the compounds, methods of making the compounds, kits comprising the compounds, and methods of using the compounds, compositions and kits for treatment of disorders associated with TREK-1, TREK-2 or both TREK-1 and TREK-2 dysfunction in a mammal.

ACTIVATOR OF TREK (TWIK RELATED K+ CHANNELS) CHANNELS

Disclosed is a compound of formula (I):

##STR00001## wherein all symbols are defined in the description. Also disclosed are pharmaceutical compositions comprising the compounds, methods of making the compounds, kits comprising the compounds, and methods of using the compounds, compositions and kits for treatment of disorders associated with TREK-1, TREK-2 or both TREK-1 and TREK-2 dysfunction in a mammal.

Methods and Compositions for Treating Fungal Infections

Provided herein are methods of treating or preventing a fungal colonisation or infection in a subject. The method includes administering a therapeutically effective amount of a compound, or a therapeutically acceptable salt thereof, to the subject, wherein the fungal colonisation or infection is caused by a fungal agent. In certain embodiments, the compound is a compound of Formula I, or a stereoisomer, tautomer, pharmaceutically acceptable salt, or prodrug thereof:

##STR00001##

Enamine compound and use thereof

Provided are a donor-acceptor type compound having a novel structure and its use. An enamine compound represented by general formula (1) ##STR00001##
(in the formula: R.sup.1 represents an electron-withdrawing group; A represents a divalent aromatic hydrocarbon group which may contain a substituent, a divalent aromatic heterocyclic group which may contain a substituent or a divalent unsaturated aliphatic hydrocarbon group which may contain a substituent; R.sup.2 represents a hydrogen atom or a hydrocarbon group which may contain a substituent; R.sup.3 and R.sup.4 are the same or different from each other and represent an aromatic hydrocarbon group which may contain a substituent or an aromatic heterocyclic group which may contain a substituent, or R.sup.3 and R.sup.4 together form an optionally substituted bicyclic aromatic heterocyclic group containing two or more nitrogen atoms or a nitrogen atom and an oxygen atom or a sulfur atom, or a tricyclic aromatic heterocyclic group which may contain a substituent; and R.sup.2 and A, or R.sup.2 and R.sup.3 may together form a cyclic structure).

Enamine compound and use thereof

Provided are a donor-acceptor type compound having a novel structure and its use. An enamine compound represented by general formula (1) ##STR00001##
(in the formula: R.sup.1 represents an electron-withdrawing group; A represents a divalent aromatic hydrocarbon group which may contain a substituent, a divalent aromatic heterocyclic group which may contain a substituent or a divalent unsaturated aliphatic hydrocarbon group which may contain a substituent; R.sup.2 represents a hydrogen atom or a hydrocarbon group which may contain a substituent; R.sup.3 and R.sup.4 are the same or different from each other and represent an aromatic hydrocarbon group which may contain a substituent or an aromatic heterocyclic group which may contain a substituent, or R.sup.3 and R.sup.4 together form an optionally substituted bicyclic aromatic heterocyclic group containing two or more nitrogen atoms or a nitrogen atom and an oxygen atom or a sulfur atom, or a tricyclic aromatic heterocyclic group which may contain a substituent; and R.sup.2 and A, or R.sup.2 and R.sup.3 may together form a cyclic structure).

Organic electroluminescent device and manufacturing method thereof

Disclosed is an organic electroluminescent device, comprising a substrate and light emitting units formed in sequence on the substrate, characterized in that, each of the light emitting units comprises a first electrode layer (1), a light emitting layer (2) and a second electrode layer (3), the light emitting layer comprises a host material and a dye, the host material is made of materials having both electron transport capability and hole transport capability; at least one material in the host material has a CT excited triplet state energy level T.sub.1 greater than its n-π excited triplet state energy level S.sub.1, and T.sub.1-S.sub.1≤0.3 eV; or, at least one material in the host material has a CT excited triplet state energy level T.sub.1 greater than its n-π excited triplet state energy level S.sub.1, and T.sub.1-S.sub.1≥1 eV, with the difference between its n-π excited second triplet state energy level and its CT excited first singlet state energy level being in the range of −0.1 eV to 0.1 eV. The organic electroluminescent device configuration can sufficiently utilize the triplet state energy in the host material and the dye to increase the luminous efficiency and prolong the service life of the device.

Organic electroluminescent device and manufacturing method thereof

Disclosed is an organic electroluminescent device, comprising a substrate and light emitting units formed in sequence on the substrate, characterized in that, each of the light emitting units comprises a first electrode layer (1), a light emitting layer (2) and a second electrode layer (3), the light emitting layer comprises a host material and a dye, the host material is made of materials having both electron transport capability and hole transport capability; at least one material in the host material has a CT excited triplet state energy level T.sub.1 greater than its n-π excited triplet state energy level S.sub.1, and T.sub.1-S.sub.1≤0.3 eV; or, at least one material in the host material has a CT excited triplet state energy level T.sub.1 greater than its n-π excited triplet state energy level S.sub.1, and T.sub.1-S.sub.1≥1 eV, with the difference between its n-π excited second triplet state energy level and its CT excited first singlet state energy level being in the range of −0.1 eV to 0.1 eV. The organic electroluminescent device configuration can sufficiently utilize the triplet state energy in the host material and the dye to increase the luminous efficiency and prolong the service life of the device.