1796-83-4Relevant academic research and scientific papers
CGRP ANTAGONIST COMPOUNDS
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Page/Page column 120-121, (2020/12/30)
The disclosures herein relate to novel compounds of Formula (1a): and salts thereof, wherein W, Z, L, R1and R2 are defined herein, and their use in treating, preventing, ameliorating, controlling or reducing the risk of disorders associated with CGRP receptors.
NON-PEPTIDE OPIOID RECEPTOR MODULATORS
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Page/Page column 15, (2020/03/15)
Non-peptide MOR opioid receptor modulators are provided. The compounds exhibit predominantly central activity and are used to treat e.g. opioid addiction. The compounds described herein are generally delivered (administered) in a pharmaceutical compositio
CGRP ANTAGONIST COMPOUNDS
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Page/Page column 40; 41, (2020/12/30)
The disclosures herein relate to novel compounds of Formula (1): and salts thereof, wherein A1, A2, Q, X, R1, R2 and R3 are defined herein, and their use in treating, preventing, ameliorating, control
Design, Synthesis, and Biological Evaluation of the Third Generation 17-Cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6β-[(4′-pyridyl)carboxamido]morphinan (NAP) Derivatives as μ/κ Opioid Receptor Dual Selective Ligands
Zheng, Yi,Obeng, Samuel,Wang, Huiqun,Jali, Abdulmajeed M.,Peddibhotla, Bharath,Williams, Dwight A.,Zou, Chuanchun,Stevens, David L.,Dewey, William L.,Akbarali, Hamid I.,Selley, Dana E.,Zhang, Yan
supporting information, p. 561 - 574 (2019/01/30)
μ opioid receptor (MOR) agonists have been widely applied for treating moderate to severe pain. However, numerous adverse effects have been associated with their application, including opioid-induced constipation (OIC), respiratory depression, and addicti
HETEROARYLDIHYDROPYRIMIDINE DERIVATIVES AND METHODS OF TREATING HEPATITIS B INFECTIONS
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Page/Page column 39; 40, (2019/01/17)
Provided herein are compounds useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject.
PIPERIDINE COMPOUNDS AS PCSK9 INHIBITORS
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Paragraph 0263; 0264; 0265, (2018/11/21)
One aspect of the invention relates to a series of new PCSK9 inhibitor compounds comprising piperidine ring structures, including compounds of formula (I) and/or pharmaceutically acceptable salts thereof. Another aspect of the invention relates to methods of treating PCSK9 receptor related diseases comprising administration of one or more compounds of formula (I) or a pharmaceutically acceptable salt thereof.
Preparation method of 2-((1S3aR7aR)-5-tert-butyloxycarbonyltetrahydrofuro[3,4]piperidine-1)acetic acid
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Paragraph 0007, (2017/12/27)
The invention relates to a preparation method of 2-((1S3aR7aR)-5-tert-butyloxycarbonyltetrahydrofuro[3,4]piperidine-1)acetic acid. The preparation method comprises 11 steps: carrying out esterification on a dicarboxylic acid piperidine compound 1 in thionyl chloride to obtain a diester compound 2; then reducing a pyridine ring by utilizing palladium carbon to obtain a compound 3; then taking the compound 3 to react with Boc acid anhydride to obtain a Boc protected compound 4; hydrolyzing the compound 4 by utilizing lithium hydroxide to obtain a dicarboxylic acid compound 5; carrying out ring closure in acetic anhydride to obtain a compound 6; carrying out reduction and ring opening by utilizing NaBH4 to obtain a mixture of position isomerism compounds 7A and 7B; carrying out the ring closure in the presence of iodomethane and potassium carbonate to generate position isomerism lactone 8A and 8B; step 8, reducing the 8A, obtained by column passing separation, by utilizing DIBAH (Diisobutylaluminum Hydride) to obtain a compound 9; carrying out Wittig reaction to obtain a compound 10; carrying out Michael addition under an alkaline condition to obtain a compound 11; finally, hydrolyzing the compound 11 under the alkaline condition to obtain a final compound.
Design, Synthesis, and Evaluation of the Highly Selective and Potent G-Protein-Coupled Receptor Kinase 2 (GRK2) Inhibitor for the Potential Treatment of Heart Failure
Okawa, Tomohiro,Aramaki, Yoshio,Yamamoto, Mitsuo,Kobayashi, Toshitake,Fukumoto, Shoji,Toyoda, Yukio,Henta, Tsutomu,Hata, Akito,Ikeda, Shota,Kaneko, Manami,Hoffman, Isaac D.,Sang, Bi-Ching,Zou, Hua,Kawamoto, Tetsuji
, p. 6942 - 6990 (2017/09/07)
A novel class of therapeutic drug candidates for heart failure, highly potent and selective GRK2 inhibitors, exhibit potentiation of β-adrenergic signaling in vitro studies. Hydrazone derivative 5 and 1,2,4-triazole derivative 24a were identified as hit compounds by HTS. New scaffold generation and SAR studies of all parts resulted in a 4-methyl-1,2,4-triazole derivative with an N-benzylcarboxamide moiety with highly potent activity toward GRK2 and selectivity over other kinases. In terms of subtype selectivity, these compounds showed enough selectivity against GRK1, 5, 6, and 7 with almost equipotent inhibition to GRK3. Our medicinal chemistry efforts led to the discovery of 115h (GRK2 IC50 = 18 nM), which was obtained the cocrystal structure with human GRK2 and an inhibitor of GRK2 that potentiates β-adrenergic receptor (βAR)-mediated cAMP accumulation and prevents internalization of βARs in β2AR-expressing HEK293 cells treated with isoproterenol. Therefore, 115h appears to be a novel class of therapeutic for heart failure treatment.
And circular PI3K inhibitors (by machine translation)
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Paragraph 0402; 0403; 0404, (2016/10/08)
The invention belongs to the field of medical technology, in particular to general formula (I) and of the everted shown in the PI3K inhibitor, or a pharmaceutically acceptable salt, ester, stereo isomers, solvates, wherein R 1, R 2, R 3 as defined in the specification. The invention also relates to methods of preparing such compounds, pharmaceutical formulations containing these compounds and pharmaceutical compositions, use of these compounds in the preparation and treatment and/or prevention of proliferative diseases of application of the medicament. (by machine translation)
