- BICYCLIC INHIBITORS OF ALK
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The present invention relates to compounds of formula (1) or pharmaceutical acceptable salts, Formula (1) wherein R1, R2, R3, X, Y, Z, A, B, G1, m, and n are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as ALK and methods of treating diseases such as cancer.
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Paragraph 0375
(2014/06/25)
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- BICYCLIC INHIBITORS OF ALK
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The present invention relates to compounds of formula (1) or pharmaceutical acceptable salts, Formula (1) wherein R1, R2, R3, X, Y, Z, A, B, G1, m, and n are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as ALK and methods of treating diseases such as cancer.
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Page/Page column 90
(2012/08/07)
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- Synthesis and preliminary evaluation of curcumin analogues as cytotoxic agents
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A series of curcumin analogues with different substituents at the 4-position of the phenyl group were synthesized and screened for in vitro cytotoxicity against a panel of human cancer cell lines. Several novel curcumin analogues, especially 32 and 34, exhibited selective and potent cytotoxic activity against human epidermoid carcinoma cell line A-431 and human glioblastoma cell line U-251, implying their specific potential in the chemoprevention and chemotherapy of skin cancer and glioma. The preliminary SAR information extracted from the results suggested that introduction of appropriate substituents to the 4′-positions could be a promising approach for the development of new cytotoxic curcumin analogues with special selectivity for A-431 and U-251 cell lines.
- Zhang, Qin,Zhong, Ying,Yan, Lin-Na,Sun, Xun,Gong, Tao,Zhang, Zhi-Rong
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scheme or table
p. 1010 - 1014
(2011/03/21)
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- QUINOLONE CARBOXYLIC ACID DERIVATIVES FOR TREATMENT OF HYPERPROLIFERATIVE CONDITIONS
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Quinolone carboxylic acid derivatives of formula (I) wherein Ar is an optionally substituted phenyl, pyridyl, or pyrimidinyl group and the substituent groups R1, R4, R10, R11, R19, and R20 are as defined in the specification, pharmaceutical compositions containing them, and methods of using them in treatment of hyperproliferative diseases such as cancer are disclosed and claimed.
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Page/Page column 124-125
(2010/02/14)
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- Trifluoromethyl-substituted hydantoins, versatile building blocks for rational drug design
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Preparatively simple, one-pot syntheses of trifluoromethyl-substituted hydantoins starting from Boc-protected imines of hexafluoroacetone and trifluoropyruvate are described. They represent valuable building blocks for the construction of constrained pept
- Wehner, Volkmar,Stilz, Hans-Ulrich,Osipov, Sergej N.,Golubev, Alexander S.,Sieler, Joachim,Burger, Klaus
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p. 4295 - 4302
(2007/10/03)
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- Heterocyclic compounds as bradykinin antagonists
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This invention relates to a compound of the formula: wherein A1is lower alkylene, R1is substituted quinolyl, etc., R2is hydrogen, halogen or lower alkyl, R3is halogen or lower alkyl, and R4is a group
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Page column 22
(2010/02/04)
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- Benzimidazole compounds as bradykinin antagonists
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PCT No. PCT/JP95/01478 Sec. 371 Date Feb. 3, 1997 Sec. 102(e) Date Feb. 3, 1997 PCT Filed Jul. 25, 1995 PCT Pub. No. WO96/04251 PCT Pub. Date Feb. 15, 1996This invention relates to a heterocyclic compound of the formula: wherein a group of the formula: is a group of the formula: etc., X is O, S or N-R5, R1 is lower alkyl, etc., R5 is hydrogen, lower alkyl, etc., R2 is hydrogen, halogen, lower alkyl, etc., R3 is halogen, lower alkyl, etc., R4 is amino optionally having suitable substituent(s), and A is lower alkylene, and a salt thereof, to processes for preparation thereof, and to a pharmaceutical composition comprising the same for the prevention and/or the treatment of bradykinin or its analogues mediated diseases in human being or animals.
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- Pyridopyrimidones, quinolines and fused N-heterocycles as bradykinin antagonists
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This invention relates to a compound of the formula: STR1 wherein Z is a group of the formula: STR2 in which X1 is N or C--R1, X2 is N or C--R9, X3 is N or C--R2, R1 is lower alk
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- Heterocyclic compounds as bradykinin antagonists
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This invention relates to a compound of formula (I) wherein A1 is lower alkylene, R1 is substituted quinolyl, etc., R2 is hydrogen, halogen or lower alkyl, R3 is halogen or lower alkyl, and R4 is a gr
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- Key intermediates in cyclotriveratrylene chemistry. Synthesis of new C3-cyclotriveratrylenes with nitrogen substituents
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Cyclotriveratrylenes 2 and 3 bear amido substituents at the periphery of the ring and were obtained in 95-97percent yield by cyclodehydration of the 3-methoxy-4-acetamidobenzyl alcohol derivatives 6 and 7.Upon reaction with sodium peroxide, 2 and 3 gave t
- Garcia, C.,Malthete, J.,Collet, A.
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