637336-53-9Relevant academic research and scientific papers
Piperidine compound and preparation method and medical application thereof
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Paragraph 0296-0300; 0302, (2021/04/07)
The invention discloses a piperidine compound shown as a formula (I) and a preparation method and medical application thereof, and particularly relates to a piperidine USP7 inhibitor compound or pharmaceutically acceptable salt or ester or solvate thereof and a preparation method and application of the piperidine USP7 inhibitor compound or pharmaceutically acceptable salt or ester or solvate thereof. The compound provided by the invention can inhibit the activity of USP7 enzyme, has very good selectivity and druggability, and can be used for preparing medicines for preventing or treating tumor diseases or virus infectious diseases.
N-benzylpiperidinol derivatives as novel USP7 inhibitors: Structure–activity relationships and X-ray crystallographic studies
Chen, Caiping,Chen, Hui,Cheng, Keguang,Li, Minglei,Liu, Jun,Liu, Shengjie,Sun, Hongbin,Wang, Yue,Wen, Xiaoan,Xu, Qing-Long,Yuan, Haoliang,Zhou, Jin,Zhou, Shuxi,Zhou, Xinyu
supporting information, (2020/06/03)
USP7 as a deubiquitinase plays important roles in regulating the stability of some oncoproteins including MDM2 and DNMT1, and thus represents a potential anticancer target. Through comparative analysis of USP7 co-crystal structures in complex with the rep
Design, Synthesis, and Physicochemical and Pharmacological Profiling of 7-Hydroxy-5-oxopyrazolo[4,3-b]pyridine-6-carboxamide Derivatives with Antiosteoarthritic Activity in Vivo
Mugnaini, Claudia,Kostrzewa, Magdalena,Bryk, Marta,Mahmoud, Ali Mokhtar,Brizzi, Antonella,Lamponi, Stefania,Giorgi, Gianluca,Ferlenghi, Francesca,Vacondio, Federica,MacCioni, Paola,Colombo, Giancarlo,Mor, Marco,Starowicz, Katarzyna,Di Marzo, Vincenzo,Ligresti, Alessia,Corelli, Federico
, p. 7369 - 7391 (2020/09/12)
The hallmark of joint diseases, such as osteoarthritis (OA), is pain, originating from both inflammatory and neuropathic components, and compounds able to modulate the signal transduction pathways of the cannabinoid type-2 receptor (CB2R) can represent a helpful option in the treatment of OA. In this perspective, a set of 18 cannabinoid type-2 receptor (CB2R) ligands was developed based on an unprecedented structure. With the aim of improving the physicochemical properties of previously reported 4-hydroxy-2-quinolone-3-carboxamides, a structural optimization program led to the discovery of isosteric 7-hydroxy-5-oxopyrazolo[4,3-b]pyridine-6-carboxamide derivatives. These new compounds are endowed with high affinity for the CB2R and moderate to good selectivity over the cannabinoid type-1 receptor (CB1R), associated with good physicochemical characteristics. As to the functional activity at the CB2R, compounds able to act either as agonists or as inverse agonists/antagonists were discovered. Among them, compound 51 emerged as a potent CB2R agonist able to reduce pain in rats carrying OA induced by injection of monoiodoacetic acid (MIA).
2-AZABICYCLO[3.1.1] DERIVATIVES AS ANTAGONISTS OF THE OREXIN-1 AND OREXIN-2 RECEPTORS
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Page/Page column 78, (2019/05/15)
There is provided a compound of formula I, wherein L1, R1, R2, R5, X, A and B have meanings given in the description, and pharmaceutically acceptable salts, solvates and prodrugs thereof, which compounds are useful as antagonists of the orexin-1 and orexin-2 receptors or as selective antagonists of the orexin-1 receptor, and thus, in particular, in the treatment or prevention of inter alia substance dependence, addiction, anxiety disorders, panic disorders, binge eating, compulsive disorders, impulse control disorders, cognitive impairment and Alzheimer's disease.
IRAK DEGRADERS AND USES THEREOF
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Paragraph 3146; 3147, (2019/07/10)
The present invention provides compounds, compositions thereof, and methods of using the same.
SUBSTITUTED 2-AZABICYCLO[3.1.1]HEPTANE AND 2-AZABICYCLO[3.2.1]OCTANE DERIVATIVES AS OREXIN RECEPTOR ANTAGONISTS
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Page/Page column 127, (2019/03/17)
There is provided a compound of formula (I), wherein L1 to L3, R1 to R4, X, A and B have meanings given in the description, and pharmaceutically acceptable salts, solvates and prodrugs thereof, which compounds are useful as antagonists of the orexin-1 and orexin-2 receptors or as selective antagonists of the orexin-1 receptor, and thus, in particular, in the treatment or prevention of inter alia substance dependence, addiction, anxiety disorders, panic disorders, binge eating, compulsive disorders, impulse control disorders, cognitive impairment and Alzheimer's disease.
Pyrazolo[4,3-d]pyrimidines as Antitumor Agents
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Paragraph 0048, (2019/09/20)
A compound of Formula I, or optionally a salt or a hydrate of the compound of Formula I is provided: wherein X is one selected from the group consisting of wherein R is an alkyl group having from one to six carbon atoms, and wherein R2 is a halogen atom. A pharmaceutical composition comprising a compound of Formula I, or optionally a salt or a hydrate of the compound of Formula I, and a pharmaceutically acceptable carrier, is provided. A method of treating a patient with cancer is set forth including administering a therapeutically acceptable amount of the compound of Formula I, or a salt or a hydrate of the compound of Formula I, or a pharmaceutical composition comprising a compound of Formula I.
HETEROCYCLIC COMPOUND
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Paragraph 0294, (2018/03/25)
The present invention relates to a compound which can be useful for the treatment or prevention of SPT-related diseases including cancer and congenital diseases associated with sphingolipid accumulation (including Niemann-Pick disease).
BENZODIAZEPINE DERIVATIVES AS RSV INHIBITORS
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Page/Page column 157, (2017/02/09)
The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit Respiratory Syncytial Virus (RSV). The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from RSV infection. The invention also relates to methods of treating an RSV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
Pyrazolecarboxamide derivatives and application thereof
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Paragraph 0130-0133, (2017/10/23)
The invention relates to pyrazolecarboxamide derivatives or pharmaceutically acceptable salt or precursors thereof. The structure of the pyrazolecarboxamide derivatives is shown in the general formula (I) in the specification, wherein R1 is selected from
