89399-17-7Relevant articles and documents
Heterocyclic compound as well as preparation method and medical application thereof
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Paragraph 0213-0216; 0222-0226, (2021/01/11)
The invention relates to a heterocyclic compound suitable for inhibiting or regulating Janus family kinase (JAK), in particular tyrosine kinase 2 (TYK2), a preparation method of the heterocyclic compound and application of the heterocyclic compound in medicine. Specifically, the present invention relates to a compound represented by a general formula (I), a pharmaceutically acceptable salt thereof, a pharmaceutical composition containing the compound or the pharmaceutically acceptable salt thereof, and a method of using the compound or the pharmaceutically acceptable salt thereof to treat and/or prevent Janus kinase-mediated related diseases, especially autoimmune diseases, inflammatory diseases and cancers and a method for preparing the compound or pharmaceutically acceptable salt thereof. The invention also relates to application of the compound or the pharmaceutically acceptable salt thereof or the pharmaceutical composition containing the compound or the pharmaceutically acceptablesalt thereof in preparation of drugs for treating and/or preventing Janus kinase mediated related diseases, especially autoimmune diseases, inflammatory diseases and cancers. Each substituent of thegeneral formula (I) is as defined in the specification.
HETEROCYCLIC COMPOUNDS FOR MEDIATING TYROSINE KINASE 2 ACTIVITY
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Page/Page column 44; 45, (2021/01/23)
Heterocyclic compounds shown in Formula (I) suitable for inhibiting or regulating the activity of Janus kinase (JAK), particularly tyrosine kinase 2 (TYK2). The compounds are useful for preventing and/or treating relevant JAK-mediated diseases, such as autoimmune diseases, inflammatory diseases, and cancers.
Heterogeneous Iron-Catalyzed Hydrogenation of Nitroarenes under Water-Gas Shift Reaction Conditions
Ryabchuk, Pavel,Junge, Kathrin,Beller, Matthias
supporting information, p. 4369 - 4376 (2018/11/21)
Reduction of various nitroarenes in the presence of heterogeneous iron oxide-based catalyst Fe 2 O 3 /NGr@C under water-gas shift reaction (WGSR) conditions has been demonstrated. The catalytic material is prepared in a straightforward manner via deposition/pyrolysis of iron-phenanthroline complex on carbon support. It shows high chemoselectivity towards the reduction of nitroarenes in the presence of other reducible and/or poisoning-capable functional groups. Hydrogenation is achieved using CO/H 2 O as a hydrogen source. Furthermore, it is demonstrated that the presence of triethylamine additive has a significant positive effect on the rate of reduction.
Drug evolution concept in drug design: 1. Hybridization method
Lazar, Carmen,Kluczyk, Alicja,Kiyota, Taira,Konishi, Yasuo
, p. 6973 - 6982 (2007/10/03)
A novel concept, "drug evolution", is proposed to develop chemical libraries that have a high probability of finding drugs or drug candidates. It converts biological evolution into chemical evolution. In this paper, we present "hybridization" drug evolution, which is the equivalent of sexual recombination of parental genomes in biological evolution. The hybridization essentially shuffles the building blocks of the parent drugs and ought to drug(s); no drug evolution can otherwise occur. We hybridized two drugs, benzocaine and metoclopramide and generated 16 molecules that include the parent drugs, four known drugs, and two molecules whose therapeutic activities are reported. The unusually high number of drugs and drug candidates in the library encourages high expectations of finding new drug(s) or drug candidate(s) within the remaining eight compounds. Interestingly, the therapeutic applications of the eight drugs or drug candidates in the library are fairly diverse as 38 therapeutic applications and 25 molecular targets are counted. Therefore, the library fits as a general chemical library for unspecified therapeutic activities. The hybridization of other two drugs, aspirin and cresotamide, is also described to demonstrate the generality of the method.
Anticonvulsant activity of some 4-aminobenzamides
Clark,Wells,Sansom,et al.
, p. 779 - 782 (2007/10/02)
A series of 4-aminobenzamides of some simple primary and secondary amines were prepared and evaluated for anticonvulsant effects. The compounds were tested in mice against seizures induced by electroshock and pentylenetetrazole (metrazole) and in the rotorod assay for neurologic deficit. For those N-alkyl amides tested, 4-amino-N-amylbenzamide was the most potent against maximal electroshock seizures (MES): ED50=42.98 mg/kg; however, the N-cyclohexylbenzamide showed the greatest protective index (PI=TD50/ED50), 2.8. The introduction of a second aromatic ring produced more potent compounds, with d,l-4-amino-N-(α-methylbenzyl)-benzamide showing the highest level of activity. This compound has an anti-MES ED50 of 18.02 mg/kg in mice when administered intraperitoneally (ip) and a TD50 of 170.78 mg/kg (PI=9.5) in the same species. These data compare quite favorably with those for phenobarbital and phenytoin in the same assays.