178311-48-3Relevant articles and documents
Compound with degrading STAT3 enzyme and preparation method and pharmaceutical application thereof
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Paragraph 0574; 0577; 0583-0587, (2021/10/27)
The present invention relates to a compound represented by general formula (I) or a stereoisomer thereof. Use of deuterated, solvates, prodrugs, metabolites, pharmaceutically acceptable salts or co-crystals, and intermediates and preparation methods, and in STAT3-related diseases such as tumors. B-L-K(I).
3-Azetidinylalkylpiperidines or -pyrrolidines as tachykinin antagonists
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, (2008/06/13)
The present invention provides compounds of formula (I) and the pharmaceutically acceptable salts thereof. Such compounds and salts are tachykinin antagonists.
3-aza and 3-oxa piperidone tachykinin antagonists
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, (2008/06/13)
Compounds of the formula: STR1 wherein: X is O, NH or NR1 ; R1 is C1 -C6 alkyl, C3 -C7 cycloalkyl, C3 -C7 cycloalkyl(C1 -C4)alkyl, aryl or aryl (C1 -C4)alkyl; wherein the C1 -C6 alkyl group is optionally substituted by fluorine and the C3 -C7 cycloalkyl or C3 -C7 cycloalkyl(C1 -C4 )alkyl group is optionally substituted in the cycloalkyl ring by up to two substituents each independently selected from halo, C1 -C4 alkoxy or halo(C1 -C4)alkoxy; R2 is phenyl optionally substituted with one or two halo substituents, indolyl or thienyl; R3 is NH2, --NR4 SO2 (C1 -C6 alkyl), --NR4 SO2 aryl, --NR4 CO(C1 -C6 alkyl), --NR4 CO aryl or a 5 to 7-membered N-linked cyclic group incorporating W in the ring wherein W is O, NR5, CH(OH), CHCO2 H, CHN(R4)2, CHF, CF2, C=O or CH2 ; R4 is H or C1 -C6 alkyl; R5 is H, C1 -C6 alkyl, C3 -C7 cycloalkyl, C3 -C7 cycloalkyl(C1 -C6)alkyl, C2 -C6 alkanoyl, C4 -C8 cycloalkanoyl, C3 -C7 cycloalkyl(C2 -C6)alkanoyl, aryl CO--, C1 -C6 alkyl SO2 --, C3 -C7 cycloalkyl SO2 --, C3 -C7 cycloalkyl(C1 -C6)alkyl SO2 --, aryl-SO2 -- or (R6)2 NSO2 --, wherein each R6 is independently H or C1 -C4 alkyl or the two groups may be joined to form with the nitrogen atom to which they are attached, a pyrrolidinyl, piperidino, morphlino or piperazinyl group; m is 0, 1 or 2 with the proviso that m is not 0 when W is NR5, C=O, or O; and n is an integer of from 1 to 4; are neurokinin receptor antagonists of utility in the treatment of a variety of medical conditions including urinary incontinence, asthma and related conditions.