- 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; 0667
(2017/02/28)
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- Discovery of Ro 48-5695: A potent mixed endothelin receptor antagonist optimized from Bosentan
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Implementation of a pyridylcarbamoyl group and an isopropylpyridylsulfonamide substituent as key components in the scaffold of Bosentan resulted in the identification of the potent orally active endothelin receptor antagonist Ro 48-5695. It shows affinities for ET(A) and ET(B) receptors in the low nanomolar range and high functional antagonistic potency in vitro.
- Neidhart, Werner,Breu, Volker,Burri, Kaspar,Clozel, Martine,Hirth, Georges,Klinkhammer, Uwe,Giller, Thomas,Ramuz, Henri
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p. 2223 - 2228
(2007/10/03)
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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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