Patent classifications
C07F9/655354
SUBSTITUTED CONDENSED THIOPHENES AS MODULATORS OF STING
A compound of formula (I):
##STR00001##
wherein: R.sup.1 is selected from (i) H, (ii) C.sub.3-6cycloalkyl, (iii) C.sub.3-7heterocyclyl optionally substituted with a group selected from: methyl and ester, and (iv) linear or branched C.sub.1-4alkyl optionally substituted with a group selected from: alkoxy, amino, amido, acylamido, acyloxy, alkyl carboxyl ester, alkyl carbamoyl, alkyl carbamoyl ester, phenyl, phosphonate ester, C.sub.3-7heterocyclyl optionally substituted with a group selected from methyl and oxo, and a naturally occurring amino acid, optionally N-substituted with a group selected from methyl, acetyl and boc; A.sup.1 is CR.sup.A or N; A.sup.2 is CR.sup.B or N; A.sup.3 is CR.sup.C or N; A.sup.4 is CR.sup.D or N; where no more than two of A.sup.1, A.sup.2, A.sup.3, and A.sup.4 may be N; one or two of R.sup.A, R.sup.B, R.sup.C, and R.sup.D, (if present) are selected from H, F, Cl, Br, Me, CF.sub.3, cyclopropyl, cyano, OMe, OEt, CH.sub.2OH, CH.sub.2OMe and CH.sub.2NMe.sub.2; the remainder of R.sup.A, R.sup.B, R.sup.C, and R.sup.D, (if present) are H; Y is O, NH or CH.sub.2; R.sup.Y is selected from: (RYA) and (RYB).
Substituted condensed thiophenes as modulators of sting
A compound of formula (I), wherein R.sup.1 is selected from (i) H, (ii) C.sub.3-6cycloalkyl, (iii) C.sub.3-7heterocyclyl optionally substituted with a group selected from: methyl and ester, and (iv) linear or branched C.sub.1-4alkyl optionally substituted with a group selected from: alkoxy, amino, amido, acylamido, acyloxy, alkyl carboxyl ester, alkyl carbamoyl, alkyl carbamoyl ester, phenyl, phosphonate ester, C.sub.3-7heterocyclyl optionally substituted with a group selected from methyl and oxo, and a naturally occurring amino acid, optionally N-substituted with a group selected from methyl, acetyl and boc; A.sup.1 is CR.sup.A or N; A.sup.2 is CR.sup.B or N; A.sup.3 is CR.sup.C or N; A.sup.4 is CR.sup.D or N; where no more than two of A.sup.1, A.sup.2, A.sup.3, and A.sup.4 may be N; one or two of R.sup.A, R.sup.B, R.sup.C, and R.sup.D, (if present) are selected from H, F, Cl, Br, Me, CF.sub.3, cyclopropyl, cyano, OMe, OEt, CH.sub.2OH, CH.sub.2OMe and CH.sub.2NMe.sub.2; the remainder of R.sup.A, R.sup.B, R.sup.C, and R.sup.D, (if present) are H; Y is O, NH or CH.sub.2; R.sup.Y is selected from: (RYA) and (RYB).
Enhancing CD8+ T cells for adoptive T cell therapy by inhibiting PTPN1 (PTP1B) and PTPN2 (TC-PTP)
The invention encompasses ex vivo method of stimulating isolated memory T-cell, tumor-infiltrating lymphocyte (TIL), T cell receptor (TCR) engineered cell, and/or chimeric antigen receptor (CAR) engineered cell with compounds of Formula I below, which are inhibitors of the TC-PTP enzyme. ##STR00001##
SMALL MOLECULE STAT PROTEIN DEGRADERS
The present disclosure provides compounds represented by Formula (I) and the pharmaceutically acceptable salts and solvates thereof, wherein R.sup.1a, R.sup.1b, R.sup.3a, R.sup.4, A, E.sup.1, E.sup.2, M, and Q are as set forth in the specification. Compounds of Formula (I) are STAT protein degraders and thus are useful for the treatment of cancer and other diseases.
##STR00001##
DIMERIC COMPOUNDS AS STING AGONISTS
The present disclosure relates to dimeric STING agonists of Formulae (I), (II), (III), (IV), (V), and (VI), and pharmaceutically acceptable salts thereof. The present disclosure also relates to methods of preparing the compounds and methods of using the compounds.
Compound, light emitting material, and organic light emitting device
The compound represented by the following general formula is useful as a light emitting material. Ar.sup.1 represents an arylene group, Ar.sup.2 and Ar.sup.3 represent an aryl group, and R.sup.1 to R.sup.8 represent a hydrogen atom or a substituent, provided that at least one of R.sup.1 to R.sup.8 represents a diarylamino group. ##STR00001##
Organic electroluminescent devices
The present disclosure relates to display technologies, and particularly discloses an organic electroluminescent device. This organic electroluminescent device includes a light-emitting layer, the light-emitting includes an exciplex composed of a donor molecule and an acceptor molecule, and a wide band gap material for increasing the inter-molecular spacing between the donor molecule and the acceptor molecule. According to the device of the present disclosure, the degree of orbital overlap of HOMO and LUMO of the formed exciplex and the singlet-triplet energy level difference can be reduced, the reverse intersystem crossing rate (k.sub.RISC) of the exciplex host can be increased, the Föster energy transferred to the guest molecule can be enhanced, and the efficiency and the lifetime of the device can be improved.
Methods and compositions for inhibition of STAT3
In one aspect, the disclosure relates to prodrug compositions of a STAT inhibitor compound. In some aspects, the STAT is STAT3. Disclosed are pharmaceutical compositions comprising the prodrug inhibitors of STAT. In various aspects, the prodrug inhibitors of STAT can be used in methods of treating an inflammatory disorder, including multiple sclerosis, or a disorder of uncontrolled cellular proliferation, such as a cancer. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure.
LIGHT-EMITTING DEVICE AND ELECTRONIC APPARATUS INCLUDING THE SAME
Provided are a light-emitting device and an electronic apparatus including the same. The light-emitting device includes: a first electrode; a second electrode facing the first electrode; an interlayer located between the first electrode and the second electrode; and an electron transport capping layer located outside the second electrode, wherein the interlayer includes an emission layer and an electron transport region, one of the electron transport region and the electron transport capping layer includes a first compound represented by Formula 1, and the other one includes the first compound, a second compound represented by Formula 2, or a combination thereof, and the electron transport region further includes a metal dopant:
##STR00001## wherein, Formulae 1 and 2 are the same as described in the specification.
LIGHT-EMITTING MATERIAL INCLUDING LIGHT-EMITTING COMPOUND, LIGHT EMITTING DEVICE INCLUDING LIGHT-EMITTING MATERIAL, METHOD OF PREPARING LIGHT-EMITTING MATERIAL, AND METHOD OF PREPARING LIGHT-EMITTING COMPOUND
A light-emitting material including aminosiloxane and a light-emitting compound represented by Formula 1, a light-emitting device including the light-emitting material, a method of preparing the light-emitting material, and a method of preparing the light-emitting compound represented by Formula 1:
A.sup.1B.sup.1X.sup.1.sub.3, Formula 1 wherein A.sup.1 may be an alkali metal, B.sup.1 may be Pb, Sn, or any combination thereof, and X.sup.1 may be a halogen.