Disclosed are compounds of Formula I: ##STR00001##
or a pharmaceutically acceptable salt, a solvate, a tautomer, an isomer or a deuterated analog thereof, wherein Z.sup.2, Z.sup.3, and Z.sup.5 are as described herein, compositions thereof, and uses thereof.

The present invention relates to a process comprising converting a compound of formula (I) into a compound of formula (II) by reaction with an organolithium reagent, which compound can be further converted into duocarmycin analogs consisting of a DNA-alkylating and a DNA-binding part, and still further into corresponding antibody-drug conjugates. ##STR00001##

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-TP A-TT, PTZ-BT-TP A, NPB-TQ, TPE-TQ-A, MTPE-BTSe, DCDPP-2TP A, 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.

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-TP A-TT, PTZ-BT-TP A, NPB-TQ, TPE-TQ-A, MTPE-BTSe, DCDPP-2TP A, 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.

Substituted benzimidazole and 3H-imidazo[4,5-b]pyridines or formula I: where X and Y respectively are selected from: (i) N and N; and (ii) N and CR.sup.4; A.sup.2 is selected from: a C.sub.5 heteroarylene group, containing 2 or 3 ring heteroatoms, where the bonds to L1 and the core are to one another; L.sup.1 is selected from: (i) .sup.A1OCH.sub.2.sup.A2; (ii) .sup.A1CH.sub.2O.sup.A2; (iii) .sup.A1C(O)NH.sup.A2; (iv) .sup.A1CH(OH).sup.A2; (v) .sup.A1CH.sub.2NHC(O).sup.A2; (vi) .sup.A1SCH.sub.2.sup.A2; (vii) .sup.A1CH.sub.2S.sup.A2; (viii) .sup.A1CH.sub.2.sup.A2; and (ix) .sup.A1CH(CH.sub.3)O.sup.A2; A1 is phenyl, optionally substituted by F or CF.sub.3; their use as pharmaceuticals, and in particular, in treating cancer and hemoglobinopathies. ##STR00001##

Methods for inhibiting the growth of pancreatic cancer cells or other cancer cells driven by Sonic hedgehog are disclosed. The method involves exposing the cells to 5-acyl-6,7-dihydrothieno[3,2-c]pyridines of formula I ##STR00001##

The present invention relates to substituted triazolopyridine compounds of general formula (I): in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, and R.sup.5 are as given in the description and in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease of uncontrolled cell growth, proliferation and/or survival as well as to the use of intermediate compounds for the preparation of said compounds. ##STR00001##

The invention provides novel substituted 6-arylamino pyridone carboxamides represented by Formula I, or a pharmaceutically acceptable salt, solvate, poly-morph, ester, tautomer or prodrug thereof, and a composition comprising these compounds. The compounds provided can be used as inhibitors of MEK and are useful in the treatment of inflammatory diseases, cancer and other hyperproliferative diseases. The invention further provides a method of treatment for inflammatory diseases, cancer and other hyperproliferative diseases in mammals, especially humans. ##STR00001##

The ring-fused heterocyclic compound or a pharmaceutically acceptable salt thereof according to the present invention has a T-type calcium channel regulatory effect, and is useful, for example, as a medicament for treating and/or preventing pruritus. The present invention provides a ring-fused heterocyclic compound represented by the following general formula (I) or a pharmaceutically acceptable salt thereof and the like which has a T-type calcium channel regulatory effect and is useful as a therapeutic and/or preventive agent for pruritus, and the like. ##STR00001##
[wherein, R.sup.1 represents optionally substituted lower alkyl and the like, R.sup.2 represents optionally substituted lower alkyl and the like, R.sup.3 represents the formula (II): ##STR00002##
(wherein, n represents 0 or 1, R.sup.3a represents a hydrogen atom and the like, R.sup.3b represents a hydrogen atom and the like, and R.sup.3c represents a hydrogen atom and the like) and the like, Q represents a hydrogen atom and the like, and W.sup.1 represents a nitrogen atom and the like, W.sup.2 represents a nitrogen atom and the like].

The present invention relates to adducts between sp.sup.2 hybridized carbon allotropes and pyrrole derivatives comprising at least one sulphur atom, and crosslinkable elastomer compositions comprising such adducts. The present invention further relates to tyres for vehicle wheels comprising at least one structural element comprising a crosslinked elastomer material obtained by crosslinking of such crosslinkable elastomer compositions.