178312-50-0Relevant academic research and scientific papers
INDAZOLE COMPOUNDS AS KINASE INHIBITORS AND METHOD OF TREATING CANCER WITH SAME
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Page/Page column 89, (2013/04/25)
The present teaching provide indazole compounds represented by Structural Formulae (I) or (I') or a pharmaceutically acceptable salt thereof. Also described are pharmaceutical compositions and methods of use thereof as protein kinase inhibitors, such as T
PYRIMIDINE DERIVATIVES FOR THE TREATMENT OF ABNORMAL CELL GROWTH
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Page/Page column 86-87, (2010/11/27)
The present invention relates to a compound of the formula (I), or a pharmaceutically acceptable salt thereof, wherein Ar is a group of formula (III), and R1, R2, R13, A, K, M, L1, L2, X, Y1, Y2, Q, salt thereof, wherein R1, R2, R13, A, K, L1, L2, W, X, Z1, Z2, Y1, Y2, Z1, Z2, M, Q, W, X, m, p and q are as defined herein. Such novel pyrimidine derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. This invention also relates to a method of using such compounds in the treatment of abnormal cell growth in mammals, especially humans, and to pharmaceutical compositions containing such compounds.
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.
(Azetidin-1-ylalkyl) lactams as tachykinin antagonists
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, (2008/06/13)
The present invention provides compounds of formula (I) and the pharmaceutically acceptable salts thereof, wherein R is C3 -C7 cycloalkyl, aryl or C1 -C6 alkyl, said C1 -C6 alkyl, said C1 -C6 alkyl being optionally substituted by fluoro, COOH, --COO(C1 -C4 alkyl), C3 -C7 cycloalkyl, adamantyl, aryl or het1, and said C3 -C7 cycloalkyl being optionally substituted by 1 or 2 substituents each independently selected from C1 -C4 alkyl, C3 -C7 cycloalkyl, C1 -C4 alkoxy, hydroxy, fluoro, fluoro (C1 -C4) alkyl and fluoro (C1 -C4) Alkoxy; R1 is phenyl, naphthyl, thienyl, benzothienyl or indolyl, each optionally substituted by 1 or 2 substituents each independently selected from C1 -C4 alkyl, C1 -C4 alkoxy, halo and trifluormethyl; R2 is --CO2 H, --CONR3 R4, --CONR5 (C3 -C7 cycloalkyl), --NR5 (C2 -C5 alkanoyl), --NR3 R4, --NR5 CONR5 R6, (C3 -C7 cycloalkyl-C1 -C4 alkyl)R5 N--, --NR5 COCF3, --NR5 SO2 CF3, --NR5 (SO2 C1 -C4 alkyl), --NR5 SO2 NR5 R6, --NR5 (SO2 aryl), --N(aryl) (SO2 C1 -C4 alkyl), --OR5, --O(C3 -C7 cycloalkyl), --SO2 NR5 R6, het3 or a group of formulas: (a), (b), (c), (d), (e), (f), (g) or (h); X is C1 -C4 alkylene; X1 is a direct link or C1 -C6 alkylene; X2 is a direct link, CO, SO2, or NR5 CO; and m is 0, 1 or 2; together with intermediates used in the preparation of compositions containing and the use as tachykinin angatonists of such derivatives. STR1
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.
