- 9H-PYRIMIDO [4,5-B] INDOLES AS BET BROMODOMAIN INHIBITORS
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The present disclosure provides substituted 9H-pyrimido [4,5-b] indoles and 5H-pyrido [4,3-b] indoles and related analogs represented by Formula I and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R 1a, W, B 1, B2, G, X 1, Y1, Y2, and Y 3 are as defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula I to treat a condition or disorder responsive to inhibition of BET bromodomains such as cancer. The present disclosure is also directed to the use of compound of Formula I as synthetic intermediates.
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Paragraph 0291
(2017/05/28)
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- HEPATITIS B CORE PROTEIN ALLOSTERIC MODULATORS
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ABSTRACT The present disclosure provides, in part, compounds having allosteric effector properties against Hepatitis B virus Cp. Also provided herein are methods of treating viral infections, such as hepatitis B, comprising administering to a patient in need thereof a disclosed compound.
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Paragraph 000136
(2015/10/05)
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- Synthesis and preliminary data on new selective and potent gastric prokinetic substituted benzamides
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A series of amino-halogen-N- benzamides was synthesized and evaluated for enhancing gastric emptying.Compared to metoclopramide, domperidone and bromopride, a number of compounds were shown to be more active in enhancing gastric motility (rat stomach emptying), devoid of dopaminergic D2-receptor antagonism (rat apomorphine test) and to be less toxic. substituted benzamides / gastrokinetic activity
- Corona, L Del,Signorelli, G,Pinzetta, A,Coppi, G
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p. 419 - 425
(2007/10/02)
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