171049-42-6Relevant articles and documents
Photocatalyzed Csp3-Csp3cross-dehydrogenative coupling of: N -Boc-tetrahydroisoquinolines with α,β-unsaturated ketones
Ao, Na-Ri-Mei,Zhu, Xue-Qing,Zhao, Chun-Xin,Gao, Ya-Ru,Wang, Yong-Qiang
, p. 4752 - 4759 (2021)
A novel photocatalyzed cross-dehydrogenative coupling reaction of N-Boc-tetrahydroisoquinolines with α,β-unsaturated ketones has been developed. This research provides an easy access to a variety of C1-substituted tetrahydroisoquinolines, which can be further transformed into benzo[a]-quinolizine-2-ones, the skeletons of natural products with a wide range of biological activities. The load of the photocatalyst is low and the oxidant is inexpensive and less toxic.
Lithioarene Cycliacylation and Pd-Catalyzed Aminoethylation/Cyclization to Access Electronically Diverse Saturated Isoquinoline Derivatives
Altenbach, Robert J.,Buchman, Marek,Farney, Elliot P.,Gfesser, Gregory A.,Greszler, Stephen N.,Voight, Eric A.
, p. 776 - 789 (2022/01/14)
We report operationally facile methods for the synthesis of substituted dihydroisoquinolinones and tetrahydroisoquinolines from readily accessible o-bromobenzyl bromides and o-bromobenzaldehydes, respectively. While classical electrophilic aromatic substitution reactions are tailored to the construction of saturated isoquinolines derived from electron-rich precursors, we demonstrate efficient syntheses from electronically diverse substrates to produce cyclized products as single regioisomers.
HETEROARYL COMPOUNDS AS INHIBITORS OF PROGRAMMED NECROSIS PATHWAY, COMPOSITION AND METHOD USING THE SAME
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Paragraph 00215-00217, (2021/07/10)
The present disclosure provides heteroaryl compounds of Formula (I), processes for their preparation, pharmaceutical compositions containing them, and their use in the treatment of diseases and disorders, arising from or related to the programmed necrosis pathway.
PYRROLO [2,3-B]PYRIDINE-3-CARBOXAMIDE COMPOSITIONS AND METHODS FOR AMELIORATING HEARING LOSS
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Paragraph 00160, (2021/08/13)
N-(3-Substituted thiazol-2(3H)-ylidene)-1H-pyrrolo[2,3-b]pyridine-3-carboxamides and N-(3-substituted oxazol-2(3H)-ylidene)-1H-pyrrolo[2,3-b]pyridine-3-carboxamides (I) and (II) are disclosed. The compounds activate Yap and inhibit Lats kinases. They are therefore useful for treating hearing loss.
N-(Pyrimidin-2-yl)-1,2,3,4-tetrahydroisoquinolin-6-amine Derivatives as Selective Janus Kinase 2 Inhibitors for the Treatment of Myeloproliferative Neoplasms
Yang, Tao,Hu, Mengshi,Chen, Yong,Xiang, Mingli,Tang, Minghai,Qi, Wenyan,Shi, Mingsong,He, Jun,Yuan, Xue,Zhang, Chufeng,Liu, Kongjun,Li, Jiewen,Yang, Zhuang,Chen, Lijuan
, p. 14921 - 14936 (2020/12/22)
In this study, we described a series of N-(pyrimidin-2-yl)-1,2,3,4-tetrahydroisoquinolin-6-amine derivatives as selective JAK2 (Janus kinase 2) inhibitors. Systematic exploration of the structure-activity relationship though cyclization modification based on previously reported compound 18e led to the discovery of the superior derivative 13ac. Compound 13ac showed excellent potency on JAK2 kinase, SET-2, and Ba/F3V617F cells (high expression of JAK2V617F mutation) with IC50 values of 3, 11.7, and 41 nM, respectively. Further mechanistic studies demonstrated that compound 13ac could downregulate the phosphorylation of downstream proteins of JAK2 kinase in cells. Compound 13ac also showed good selectivity in kinase scanning and potent in vivo antitumor efficacy with 82.3% tumor growth inhibition in the SET-2 xenograft model. Moreover, 13ac significantly ameliorated the disease symptoms in a Ba/F3-JAK2V617F allograft model, with 77.1% normalization of spleen weight, which was more potent than Ruxolitinib.
1, 2 - DIHYDRO- 3H- PYRAZOLO [3, 4 - D] PYRIMIDIN -3 - ONE ANALOGS
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, (2019/02/15)
Compounds of Formula (I) are provided herein. Such compounds, as well as pharmaceutically acceptable salts and compositions thereof, are useful for treating diseases or conditions, including conditions characterized by excessive cellular proliferation, such as breast cancer.
BROAD SPECTRUM ANTIVIRAL COMPOSITIONS AND METHODS
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Page/Page column 57; 58, (2019/05/10)
Novel thiazole- and isoquinoline- containing compounds are presented that are useful for treating and/or preventing broad-spectrum viral infections. Methods of treating and/or preventing broad-specturm viral infections are also presented. These compounds have shown inhibitio of HCMV, influenza viruses, Zika virus, BK Virus and RSV replication in cell-based assays.
DIHYDROISOQUINOLINE-2(1H)-CARBOXAMIDE AND RELATED COMPOUNDS AND THEIR USE IN TREATING MEDICAL CONDITIONS
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Paragraph 000491, (2019/11/04)
The invention provides dihydroisoquinoline-2(1H)-carboxamide and related compounds, pharmaceutical compositions, and their use in the treatment of medical conditions, such as cancer, and in inhibiting HPK1 activity.
TRIAZOLOPHTHALAZINE COMPOUNDS, USE AS ANTI-HUMAN IMMUNODEFICIENCY VIRUS INHIBITORS OF HIV VIF-DEPENDENT DEGRADATION OF APOBEC3
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Paragraph 00407, (2019/07/17)
The present disclosure is concerned with triazolophthalazine compounds that are capable of inhibiting infection by the Human Immunodeficiency Virus (HIV) by inhibiting HIV Vif-dependent degradation of the APOBEC3 innate immune system. The present disclosu
HETEROARYL COMPOUNDS AND USES THEREOF
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Paragraph 00534-00536, (2016/06/28)
The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same. It has now been found that compounds of this invention, and pharmaceutically acceptable compositions thereof, are effective as inhibitors of one or more protein kinases. Such compounds have general formula I or a pharmaceutically acceptable salt thereof, wherein Ring A, Ring B, W, Ry, R3 and R4 are as defined herein.
