The present invention relates to heteroaromatic derivatives for use as a regulator, a preparation method therefor and a use thereof. In particular, disclosed are compounds represented by general formula (I), preparation methods therefor, pharmaceutical compositions comprising said compounds, and a use thereof as Janus kinase inhibitors in treating inflammatory diseases and tumor-related diseases.

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A compound of Formula I,

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is disclosed. In Formula I, M is Pd or Pt; each of X.sup.1 to X.sup.12 is C or N; each of X.sup.13 and X.sup.14 is CH, CD or N; each of Z.sup.1, Z.sup.2, and Z.sup.3 is C or N; L.sup.1 is selected from a variety of bivalent linkers; X is selected from O, S, Se, NR′, and CR″R′″; each R, R′, R.sup.1, R.sup.2, R.sup.3, R.sup.A, R.sup.B, R.sup.C, R.sup.D, and R.sup.E is hydrogen or a General Substituent; at least one of Z.sup.1, Z.sup.2, and Z.sup.3 is a carbon atom substituted with a substituent with a molecular weight of at least 16. Formulations, OLEDs, and consumer products that include Formula I are also disclosed.

A compound of Formula I,

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is disclosed. In Formula I, M is Pd or Pt; each of X.sup.1 to X.sup.12 is C or N; each of X.sup.13 and X.sup.14 is CH, CD or N; each of Z.sup.1, Z.sup.2, and Z.sup.3 is C or N; L.sup.1 is selected from a variety of bivalent linkers; X is selected from O, S, Se, NR′, and CR″R′″; each R, R′, R.sup.1, R.sup.2, R.sup.3, R.sup.A, R.sup.B, R.sup.C, R.sup.D, and R.sup.E is hydrogen or a General Substituent; at least one of Z.sup.1, Z.sup.2, and Z.sup.3 is a carbon atom substituted with a substituent with a molecular weight of at least 16. Formulations, OLEDs, and consumer products that include Formula I are also disclosed.

The present invention relates to a conjugate of a cytotoxic drug/molecule to a cell-binding molecule with a bis-linker (a dual-linker) containing a 2,3-diaminosuccinyl group. It also relates to preparation of the conjugate of a cytotoxic drug/molecule to a cell-binding molecule with the bis-linker, particularly when the drug having functional groups of amino, hydroxyl, diamino, amino-hydroxyl, dihydroxyl, carboxyl, hydrazine, aldehyde and thiol for conjugation with the bis-linker in a specific manner, as well as the therapeutic use of the conjugates.

The present invention relates to a conjugate of a cytotoxic drug/molecule to a cell-binding molecule with a bis-linker (a dual-linker) containing a 2,3-diaminosuccinyl group. It also relates to preparation of the conjugate of a cytotoxic drug/molecule to a cell-binding molecule with the bis-linker, particularly when the drug having functional groups of amino, hydroxyl, diamino, amino-hydroxyl, dihydroxyl, carboxyl, hydrazine, aldehyde and thiol for conjugation with the bis-linker in a specific manner, as well as the therapeutic use of the conjugates.

Disclosed herein are compounds of formula (I) which are inhibitors of an IDO enzyme: (I). Also disclosed herein are uses of the compounds in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising these compounds. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.

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Inhibition of indoleamine 2,3-dioxygenase (IDO1) is an attractive immunotherapeutic approach for the treatment of a variety of cancers. Dysregulation of this enzyme has also been implicated in other severe diseases such as Alzheimer's disease and arthritis. Small molecule inhibitors of Formula (Ia) and (Ib) of IDO, their synthesis, and uses thereof are provided. ##STR00001##

Inhibition of indoleamine 2,3-dioxygenase (IDO1) is an attractive immunotherapeutic approach for the treatment of a variety of cancers. Dysregulation of this enzyme has also been implicated in other severe diseases such as Alzheimer's disease and arthritis. Small molecule inhibitors of Formula (Ia) and (Ib) of IDO, their synthesis, and uses thereof are provided. ##STR00001##

The present disclosure novel pyrazine compounds targeting adenosine receptors (especially A1 and A2, particularly A2a). The present disclosure also relates to pharmaceutical compositions comprising one or more of the compounds as an active ingredient, and use of the compounds in the treatment of adenosine receptor (AR) associated diseases, for example cancer such as NSCLC, RCC, prostate cancer, and breast cancer.

The present disclosure relates to compounds of Formula (I), (II), or (III) ##STR00001## as compounds capable of emitting delayed fluorescence, and uses of these compounds in organic light-emitting diodes.