C07F9/655354

TC-PTP inhibitors as APC activators for immunotherapy

The invention encompasses the novel class of compounds represented by the Formula (I) below, which are inhibitors of the TC-PTP enzyme. The invention also encompasses pharmaceutical compositions which include the compounds shown above and methods of treating or preventing TC-PTP mediated diseases, including cancer, via their use in the activation of antigen-presenting cells, like dendritic cells, for applications in the immunotherapeutic treatment of diseases. ##STR00001##

SUBSTITUTED BENZOTHIOPHENE DERIVATIVES AND METHODS OF USE THEREOF

Provided are novel Substituted Thiophene Derivatives of Formula (I) and pharmaceutically acceptable salts thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, and R.sup.7 are as defined herein, as well as compositions comprising at least one Substituted Thiophene Derivative, and methods of using the Substituted Thiophene Derivatives for treating or preventing cancer in a patient.

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SUBSTITUTED CONDENSED THIOPHENES AS MODULATORS OF STING

A compound of formula (I):

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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).

TC-PTP INHIBITORS AS APC ACTIVATORS FOR IMMUNOTHERAPY

The invention encompasses the novel class of compounds represented by the Formula (I) below, which are inhibitors of the TC-PTP enzyme. The invention also encompasses pharmaceutical compositions which include the compounds shown above and methods of treating or preventing TC-PTP mediated diseases, including cancer, via their use in the activation of antigen-presenting cells, like dendritic cells, for applications in the immunotherapeutic treatment of diseases.

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COMPOUND, MATERIAL FOR ORGANIC ELECTROLUMINESCENT ELEMENTS, ORGANIC ELECTROLUMINESCENT ELEMENT AND ELECTRONIC DEVICE

A high-performance organic electroluminescence device and an electronic equipment provided with the organic electroluminescence device are provided. Also, a compound for achieving the organic electroluminescence device and the electronic equipment is provided. Specifically, a compound having a specific structure having a triphenylene skeleton, an organic electroluminescence device using the compound and an electronic equipment provided with the organic electroluminescence device are provided.

MITOCHONDRIOTROPIC HETEROARYL BENZAMIDE POTASSIUM CHANNEL KV1.3 INHIBITORS

The present invention relates to compounds of formula (I), processes for their preparation, and pharmaceutical compositions containing them as the active ingredient. Compounds of the present invention may be useful as mitochondrial KV1.3 inhibitors (mitoKV1.3) to treat cancer diseases and the like, including breast, colon, and prostate tumors, melanoma, smooth muscle, and skeletal muscle cancer, chronic lymphocytic leukemia, glioblastoma, and pancreatic ductal adenocarcinoma.

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PHOSPHORUS COMPOUND AND USE THEREOF

The present invention relates to a phosphorus compound and the use thereof. Specifically, provided in the present invention is a compound of formula (I), or an optical isomer, racemate, solvate, pharmaceutically acceptable salt or deuterated compound thereof. The compound of the present invention has significant and excellent precision treatment effects on tumors that have low expression, no expression, low activity or no activity of mitochondrial permeability transition pores, low expression, no expression, low activity or no activity of peptidyl prolyl isomerase F, low expression or no expression of NNMT gene, high expression of DNA methylase, high expression of UHRFI, high methylation level at a nucleotide site in NNMT gene, and/or high methylation level of DNA at CpG site in NNMT gene region.

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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##

STAT6 DEGRADERS AND USES THEREOF

The present invention provides compounds, compositions thereof, and methods of using the same.