- QUINOLINE DERIVATIVES AS SMO INHIBITORS
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Disclosed are quinoline derivatives as hedgehog pathway inhibitors, especially as SMO inhibitors. Compounds of the present invention can be used in treating diseases relating to hedgehog pathway including cancer.
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Paragraph 0665; 0666
(2017/02/28)
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- HISTONE DEMETHYLASE INHIBITORS
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The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted pyrido[3,4-d]pyrimidin-4-one derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.
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Paragraph 00253
(2016/04/09)
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- 1-Amino-4-benzylphthalazines as orally bioavailable smoothened antagonists with antitumor activity
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Abnormal activation of the Hedgehog (Hh) signaling pathway has been linked to several types of human cancers, and the development of small-molecule inhibitors of this pathway represents a promising route toward novel anticancer therapeutics. A cell-based screen performed in our laboratories identified a new class of Hh pathway inhibitors, 1-amino-4-benzylphthalazines, that act via antagonism of the Smoothened receptor. A variety of analogues were synthesized and their structure-activity relationships determined. This optimization resulted in the discovery of high affinity Smoothened antagonists, one of which was further profiled in vivo. This compound displayed a good pharmacokinetic profile and also afforded tumor regression in a genetic mouse model of medulloblastoma.
- Miller-Moslin, Karen,Peukert, Stefan,Jain, Rishi K.,McEwan, Michael A.,Karki, Rajesh,Llamas, Luis,Yusuff, Naeem,He, Feng,Li, Yanhong,Sun, Yingchuan,Dai, Miao,Perez, Lawrence,Michael, Walter,Sheng, Tao,Lei, Huangshu,Zhang, Rui,Williams, Juliet,Bourret, Aaron,Ramamurthy, Arun,Yuan, Jing,Guo, Ribo,Matsumoto, Melissa,Vattay, Anthony,Maniara, Wieslawa,Amaral, Adam,Dorsch, Marion,Kelleher III, Joseph F.
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experimental part
p. 3954 - 3968
(2010/01/16)
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- Substituted pyridyl compounds, herbicidal compositions and method of use
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Substituted pyridyl compounds, e.g. 2,6-dichloro-4(2-(2,2,2-trichloroethyl)oxiranyl) pyridine; herbicidal compositions containing such compounds and method for the control of undesired vegetation using these compositions.
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- Substituted 11-oxo-11H-pyrido[2,1-b]quinazolines and method of inhibiting allergic reactions with them
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Pyrido[2,1-b]quinazolines of the formulas STR1 wherein R1, R1 ', R2, R2 ', R3, R3 ', R4 and R10 are as hereinafter set forth, and processes for the preparation thereof
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- Pyrido[2,1-b]quinazolinecarboxylic acids as orally active antiallergy agents
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A series of 8-substituted pyrido[2,1-b]quinazoline-2-carboxylic acids was prepared by the nickel carbonyl mediated carboxylation of the corresponding bromides. The activities of these compounds in the rat PCA test are comparable to those of the corresponding 2-substituted pyrido[2,1-b]quinazoline-8-carboxylic acids.
- Tilley,LeMahieu,Carson,Kierstead,Baruth,Yaremko
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