476620-55-0Relevant articles and documents
HISTONE ACETYLTRANSFERASE (HAT) INHIBITOR AND USE THEREOF
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Paragraph 0553-0554, (2021/02/25)
The present invention relates to a histone acetyltransferase (HAT) inhibitor. Provided are a compound represented by general formula I, a pharmaceutically acceptable salt, a stereoisomer, an enantiomer, a diastereomer, an atropisomer, a racemate, a polymorph, a solvate or an isotope-labeled compound (including deuterium substitution) thereof, a preparation method therefor, a pharmaceutical composition comprising the same, and use thereof in the treatment of various HAT-related diseases or conditions.
PYRIDOPYRAZINE AND PYRIDOTRIAZINE INHIBITORS OF INFLUENZA VIRUS REPLICATION
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Paragraph 00295, (2020/05/06)
Provided herein are compounds that can inhibit the replication of influenza viruses, reduce the amount of influenza viruses, and/or treat influenza. (I)
BRIDGED TRICYCLIC CARBAMOYLPYRIDONE COMPOUNDS AND THEIR PHARMACEUTICAL USE
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Paragraph 0928, (2020/10/20)
Compounds for use in treating or preventing human immunodeficiency virus (HIV) infection are disclosed. The compounds have the following formula (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein R1, R2, L, W1, W2, X, Y, and Z are as defined herein. Methods associated with the preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
Synthesis and biological evaluation of new fluorinated and chlorinated indenoisoquinoline topoisomerase i poisons
Beck, Daniel E.,Lv, Wei,Abdelmalak, Monica,Plescia, Caroline B.,Agama, Keli,Marchand, Christophe,Pommier, Yves,Cushman, Mark
, p. 1469 - 1479 (2016/03/16)
Fluorine and chlorine are metabolically stable, but generally less active replacements for a nitro group at the 3-position of indenoisoquinoline topoisomerase IB (Top1) poisons. A number of strategies were employed in the present investigation to enhance the Top1 inhibitory potencies and cancer cell growth inhibitory activities of halogenated indenoisoquinolines. In several cases, the new compounds' activities were found to rival or surpass those of similarly substituted 3-nitroindenoisoquinolines, and several unusually potent analogs were discovered through testing in human cancer cell cultures. A hydroxyethylaminopropyl side chain on the lactam nitrogen of two halogenated indenoisoquinoline Top1 inhibitors was found to also impart inhibitory activity against tyrosyl DNA phosphodiesterases 1 and 2 (TDP1 and TDP2), which are enzymes that participate in the repair of DNA damage induced by Top1 poisons.
3,4-Diarylpiperidines as potent renin inhibitors
Lacombe, Patrick,Arbour, Mélissa,Aspiotis, Renée,Cauchon, Elizabeth,Chen, Austin,Dubé, Daniel,Falgueyret, Jean-Pierre,Fournier, Pierre-André,Gallant, Michel,Grimm, Erich,Han, Yongxin,Juteau, Hélne,Liu, Suzanna,Mellon, Christophe,Ramtohul, Yeeman,Simard, Daniel,St-Jacques, René,Tsui, Gavin Chit
scheme or table, p. 1953 - 1957 (2012/04/04)
The discovery and SAR of a series of potent renin inhibitors possessing a novel 3,4-diarylpiperidine scaffold are described herein. The resulting compound 38 exhibit low nanomolar plasma renin IC50, had a clean CYP 3A4 profile and displayed mic
PICOLINAMIDO-PROPANOIC ACID DERIVATIVES USEFUL AS GLUCAGON RECEPTOR ANTAGONISTS
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Page/Page column 68, (2012/12/13)
The present invention is directed to picolanmido-propanoic acid derivatives, pharmaceutical compositions containing them and their use in the treatment and/or prevention of disorders and conditions ameliorated by antagonizing one or more glucagon receptors, including for example metabolic diseases such as Type II diabetes mellitus and obesity.
Renin inhibitors for the treatment of hypertension: Design and optimization of a novel series of spirocyclic piperidines
Chen, Austin,Aspiotis, Renee,Campeau, Louis-Charles,Cauchon, Elizabeth,Chefson, Amadine,Ducharme, Yves,Falgueyret, Jean-Pierre,Gagne, Sebastien,Han, Yongxin,Houle, Robert,Laliberte, Sebastien,Larouche, Guillaume,Levesque, Jean-Franois,McKay, Dan,Percival, David
scheme or table, p. 7399 - 7404 (2012/02/04)
The discovery and SAR of a novel series of spirocyclic renin inhibitors are described herein. It was found that by restricting the northern aromatic plate to the bioactive conformation through spirocyclization, increase in renin potency and decrease in hE
RENIN INHIBITORS
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Page/Page column 15-16, (2011/04/13)
Renin inhibitors, which are spirocyclic piperidine amides, of structural formula (I) and pharmaceutical compositions thereof useful in the treatment of cardiovascular diseases and renal insufficiency, wherein n, for each instance in which it occurs, is independently 0, 1, or 2; R1 is hydrogen, C1-6 -alkyl or C3-6 -cycloalkyl, wherein said C1-6 -alkyl or C3-6 -cycloalkyl group can be independently substituted with 1-3 halogens; A is (i) a five- or six-membered saturated or unsaturated heterocyclic or carbocyclic monocyclic ring or (ii) a five- or six-membered saturated or unsaturated heterocyclic or carbocyclic ring which is fused to another five- or six-membered saturated or unsaturated heterocyclic or carbocyclic ring, V is a bond or -(C=O)-, -CH(OH)-, -CH2- or =CH-; U is a bond or -CH2-, or for the case when V is =CH-, U is -CH=; X is =CH-, =CF-, =C(OR3)-, or -C=O-; and Y is =CH-, =CF-, =N-, or for the case when X is -C=O-, Y is -N(R3)-.
SPIROCYCLIC PIPERIDINE DERIVATIVES USEFUL AS RENIN INHIBITORS
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Page/Page column 20; 21, (2011/06/16)
Renin inhibitors which are spirocyclic piperidine derivatives, of formula (I) and pharmaceutical compositions thereof useful in the treatment of cardiovascular diseases and renal insufficiency. or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable salt of the stereoisomer thereof, wherein: n, for each instance in which it occurs, is independently 0, 1, or 2; W is a five- or six-membered saturated or unsaturated heterocyclic or carbocyclic monocyclic ring, A is (i) a five- or six-membered saturated or unsaturated heterocyclic or carbocyclic monocyclic ring or (ii) a first five- or six-membered saturated or unsaturated heterocyclic or carbocyclic ring which is fused to a second five- or six-membered saturated or unsaturated heterocyclic or carbocyclic ring, V is -(C=O)-, -CH2- or =CH-; U is a bond or -CH2-, or, when V iS =CH-, U is-CH=; X is =CH-, =CF-, =C(OR3)-, or -(C=O)-; and Y is =CH-, =CF-, =N-, or, for the case when X is -(C=O)-, Y is -N(R3)-.
NAPHTHYLACETIC ACIDS
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Page/Page column 70, (2010/06/15)
The invention is concerned with the compounds of formula (I) and pharmaceutically acceptable salts and esters thereof, wherein X, Q, and R1-R6 are defined in the detailed description and claims. In addition, the present invention relates to methods of manufacturing and using the compounds of formula (I) as well as pharmaceutical compositions containing such compounds. The compounds of formula (I) are antagonists or partial agonists at the CRTH2 receptor and may be useful in treating diseases and disorders associated with that receptor such as asthma.