Compounds of formula (I) and its pharmaceutically acceptable salts are described ##STR00001##
wherein R.sub.1, R.sub.2, X, Y, A, B are as defined in the specification. Also disclosed are methods for preparing the compounds of formula (I) or pharmaceutically acceptable salts thereof, and pharmaceutical compositions comprising the compounds of formula (I) or pharmaceutically acceptable salts thereof.

The present invention provides novel compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and pharmaceutical compositions thereof. The present invention also provides methods and kits using the inventive compounds and pharmaceutical compositions for treating and/or preventing diseases associated with protein aggregation, such as amyloidoses (e.g., Parkinson's disease and Alzheimer's disease), treating and/or preventing neurodegenerative diseases, treating and/or preventing diseases associated with Tar DNA binding protein 43 kDa, reducing or preventing protein aggregation, and/or modulating E3 ubiquitin ligase in a subject in need thereof. ##STR00001##

The invention pertains to novel FLT3 receptor antagonists of general formula (1). The compounds are useful for the treatment or the prevention of pain disorders, cancer and autoimmune diseases.

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The invention pertains to novel FLT3 receptor antagonists of general formula (1). The compounds are useful for the treatment or the prevention of pain disorders, cancer and autoimmune diseases.

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The invention relates to a process for preparing a compound of (III) ##STR00001## wherein X is a leaving group; and R.sup.1 is C.sub.1-C.sub.6 alkyl;
which comprises oxidative rearrangement of a compound of formula (II) or a solvate thereof ##STR00002## Compounds of formula (III) are key intermediates in the synthesis of Bilastine.

The invention relates to a process for preparing a compound of (III) ##STR00001## wherein X is a leaving group; and R.sup.1 is C.sub.1-C.sub.6 alkyl;
which comprises oxidative rearrangement of a compound of formula (II) or a solvate thereof ##STR00002## Compounds of formula (III) are key intermediates in the synthesis of Bilastine.

A method for producing a nitrogen-containing fluorine-containing compound includes a step in which a compound represented by formula (5) is fluorinated to obtain a compound represented by formula (6). R.sup.3 is a single bond or a C1-20 divalent organic group. R.sup.4 and R.sup.5 are each independently a monovalent organic group having an electron-withdrawing group, a C1-20 monovalent hydrocarbon group, or a C2-20 monovalent hydrocarbon group which contains an etheric oxygen atom between carbon atoms. At least one of R.sup.4 and R.sup.5 is a monovalent organic group having an electron-withdrawing group. R.sup.3, R.sup.4, and R.sup.5 may be bonded to each other to form a divalent organic group or a trivalent organic group. R.sup.6 is a C1-20 monovalent organic group. E.sup.3 is a divalent organic group. R.sup.3F, R.sup.4F, R.sup.5F, R.sup.6F, and E.sup.3F are groups formed by fluorinating some or all of hydrogen atoms of R.sup.3, R.sup.4, R.sup.5, R.sup.6, and E.sup.3.

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A method for producing a nitrogen-containing fluorine-containing compound includes a step in which a compound represented by formula (5) is fluorinated to obtain a compound represented by formula (6). R.sup.3 is a single bond or a C1-20 divalent organic group. R.sup.4 and R.sup.5 are each independently a monovalent organic group having an electron-withdrawing group, a C1-20 monovalent hydrocarbon group, or a C2-20 monovalent hydrocarbon group which contains an etheric oxygen atom between carbon atoms. At least one of R.sup.4 and R.sup.5 is a monovalent organic group having an electron-withdrawing group. R.sup.3, R.sup.4, and R.sup.5 may be bonded to each other to form a divalent organic group or a trivalent organic group. R.sup.6 is a C1-20 monovalent organic group. E.sup.3 is a divalent organic group. R.sup.3F, R.sup.4F, R.sup.5F, R.sup.6F, and E.sup.3F are groups formed by fluorinating some or all of hydrogen atoms of R.sup.3, R.sup.4, R.sup.5, R.sup.6, and E.sup.3.

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The present invention provides NOS inhibitors such as iNOS inhibitors, or a pharmaceutically acceptable salt, ester, prodrug, complex, solvate, hydrate, or isomer thereof, in any crystalline form or in amorphous form. The inhibitors include 1,1 or 1,2 substituted-ethyl carbamimido thioates, cyclic compounds substituted with a carbamimidoyl sulfanylethylphenyl group and a carbamimidoylsulfanyl group, compounds substituted with a carbamimidoyl sulfanylethyl phenylmethyl group, bis-carbamimidoylsulfanylethyl substituted compounds, 2-propoxypyridine derivatives, alkylamine or heteroalkylamine derivatives, n-aminoethyl n-phenyl amine derivatives, and saturated heterocyclic fused benzene derivatives. Pharmaceutical products comprising the NOS inhibitors such as iNOS inhibitors and the applications thereof in prophylaxis and/or treatment of inflammatory diseases, and proliferative diseases such as cancer including gastro-intestinal, colorectal, gynecological, pancreatic, head and neck, esophageal, breast, lung, and central nervous system tumors, among others, are also provided.

It has been demonstrated that certain compounds bind to TNF and stabilise a conformation of trimeric TNF that binds to the TNF receptor. Accordingly, these compounds can be used as modulators of TNF. Anew assay for identifying compounds with this mechanism of action is also disclosed.