C07F9/655354

BENZOTHIOPHENE ESTROGEN RECEPTOR MODULATORS TO TREAT MEDICAL DISORDERS
20210171554 · 2021-06-10 · ·

This invention is a benzothiophene estrogen receptor modulator or its pharmaceutically acceptable salt, N-oxide, isotopic derivative, or prodrug thereof or a pharmaceutically acceptable composition thereof to treat an estrogen-related medical disorder. The invention also includes a combination thereof with another active agent such as a CDK inhibitor, including a CDK4/6 inhibitor, to treat a disorder mediated by the estrogen receptor, as described in more detail herein.

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.

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PHOTOSWITCHABLE DIBENZOTHIENYLMETHYL TRIPHENYLPHOSPHONIUM DERIVATIVES AND METHODS OF TREATING CANCER THEREWITH

In one aspect, the present disclosure provides a compound of the formula: In another aspect, the present disclosure also provides methods of preparing the compounds disclosed herein. In another aspect, the present disclosure also provides pharmaceutical compositions and methods of use of the compounds disclosed herein.

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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).

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Heterocyclic compound and organic light emitting diode comprising same

The present specification provides a heterocyclic compound and an organic light emitting device comprising the same.

METHODS AND COMPOSITIONS FOR INHIBITION OF STAT3
20200339525 · 2020-10-29 ·

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.

Substituted tricyclic heterocyclic compounds

Disclosed are compounds of Formula (I), Formula (II), Formula (III), and Formula (IV) or salts thereof, wherein R.sub.2 is OH or OP(O)(OH).sub.2; and R.sub.1 is defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein coupled receptor S1P.sub.1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease. ##STR00001##

ORGANIC ELECTROLUMINESCENT DEVICES
20200083461 · 2020-03-12 ·

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 Fster energy transferred to the guest molecule can be enhanced, and the efficiency and the lifetime of the device can be improved.

COMPOUND, DISPLAY PANEL, AND DISPLAY APPARATUS

Provided is a host material compound having a structure represented by Formula (I):

##STR00001## in which m and n, respectively representing the number of electron donors D and the number of electron acceptors A, are each 1, 2 or 3; p and q, respectively representing the number of the group L.sub.1 and the number of the group L.sub.2, are each 0, 1, or 2. D, L.sub.1 and L.sub.2 are each alkyl, cycloalkyl, heterocyclic group, aryl, heteroaryl, fused aryl, or fused heteroaryl; and A is selected from nitrogen-containing heterocyclic substituents, cyano-containing substituents, triaryl-boron-derived substituents, and phosphorus oxygen double bond-containing substituents. The compound has a D-()--()-A structure with bipolarity, and the bond can interrupt an intramolecular charge transfer between D and A, so that the excited state is limited to a local excited state in moiety of D or A, and the compound has a small excited-state dipole moment.

SUBSTITUTED TRICYCLIC HETEROCYCLIC COMPOUNDS

Disclosed are compounds of Formula (I), Formula (II), Formula (III), and Formula (IV) or salts thereof, wherein R.sub.2 is OH or OP(O)(OH).sub.2; and R.sub.1 is defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein coupled receptor S1P.sub.1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.

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