141872-22-2Relevant academic research and scientific papers
REGULATOR OF NITROGEN-CONTAINING HETEROAROMATIC DERIVATIVES, PREPARATION METHOD THEREFOR AND USE THEREOF
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Paragraph 0109-0113, (2021/08/27)
The present invention relates to a regulator of nitrogen-containing heteroaromatic derivatives, a preparation method therefor and the use thereof. In particular, the present invention relates to a compound as shown in the general formula (I), a preparation method therefor and a pharmaceutical composition containing the compound, and the use thereof as a protein tyrosine phosphatase-2C (SHP2) inhibitor in the treatment of diseases or conditions such as leukemia, neuroblastoma, melanoma, breast cancer, lung cancer and colorectal cancer, wherein the definition of each substituent in the general formula (I) is the same as that in the description.
NOVEL HETEROCYCLIC DERIVATIVES USEFUL AS SHP2 INHIBITORS
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Page/Page column 90, (2020/05/12)
Provided is a compound of formula I, their synthesis and their use for treating a SHP2 mediated disorder. More particularly, provided is a pharmaceutical composition comprising the said compound.
SHP2 PHOSPHATASE INHIBITORS AND METHODS OF USE THEREOF
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Paragraph 0199, (2019/10/15)
The present disclosure relates to novel compounds including formula (X) and pharmaceutical compositions thereof, and methods for inhibiting the activity of SHP2 phosphatase with the compounds and compositions of the disclosure. The present disclosure further relates to, but is not limited to, methods for treating disorders associated with SHP2 deregulation with the compounds and compositions of the disclosure.
BICYCLIC COMPOUNDS AS ALLOSTERIC SHP2 INHIBITORS
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Paragraph 00705, (2018/08/20)
The present disclosure is directed to inhibitors of SHP2 and their use in the treatment of disease. Also disclosed are pharmaceutical compositions comprising the same.
2,5-DISUBSTITUTED 3-METHYL PYRAZINES AND 2,5,6-TRISUBSTITUTED 3-METHYL PYRAZINES AS ALLOSTERIC SHP2 INHIBITORS
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Paragraph 0493, (2018/03/26)
The present disclosure is directed to inhibitors of SHP2 and their use in the treatment of disease. Also disclosed are pharmaceutical compositions comprising the same.
FUSED HETEROCYCLIC RING DERIVATIVE AND USE THEREOF
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Page/Page column 86, (2012/07/14)
The present invention provides a fused heterocycle derivative having a strong Smo inhibitory activity, and use thereof. Specially, the present invention relates to a compound represented by the formula wherein each symbol is as defined in the specification, or salt thereof, and a medicament containing the compound or a prodrug thereof, which is an Smo inhibitor or an agent for the prophylaxis or treatment of cancer.
2-(Alkylamino)nicotinic Acid and Analogs. Potent Angiotensin II Antagonists
Winn, Martin,De, Biswanath,Zydowsky, Thomas M.,Altenbach, Robert J.,Basha, Fatima Z.,et al.
, p. 2676 - 2688 (2007/10/02)
A series of pyridines and other six-membered ring heterocycles connected to a biphenyltetrazole with a-CH2-NR'-link (1) were discovered to be potent angiotensin II antagonists.In the pyrimidine carboxylic acid series (W = CR, X = N, Y = CH, Z = COOH), compounds with an alkyl group (R') on the exocyclic nitrogen were much more potent than compounds with an alkyl group (R) on the heterocyclic ring.The corresponding pyridine, pyridazine, pyrazine, and 1,2,4-triazine carboxylic acids also showed potent in vitro angiotensin II antagonism.The pyridine (W, X, Y = CH, Z = COOH, R' = n-C3H7) demonstrated potent in vitro activity (pA2 = 10.10, rabbit aorta, and Ki = 0.61 nM, receptor binding in rat liver) as well as exceptional oral antihypertensive activity and bioavailability.Any nonacidic replacement for the carboxylic acid was detrimental for activity.
Angiotensin II receptor antagonists
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, (2008/06/13)
Compounds are disclosed having the formula: STR1 The compounds of the invention are angiotensin II receptor antagonists.
