261732-38-1Relevant articles and documents
Allyl amine compound and application thereof
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, (2020/08/12)
The invention belongs to the technical field of medicines, and particularly relates to an allyl amine compound shown as a formula I or pharmaceutically acceptable salt, ester, stereoisomer and tautomer thereof, wherein R1, R2, R3, R4, R5, R6, L1 and Cy1 are defined in the specification. The invention also relates to pharmaceutical preparations and pharmaceutical compositions containing the compound, and application of the compound in prevention and/or treatment of diseases related to SSAO/VAP-1 protein or mediated by the SSAO/VAP-1 protein.
4-aminopyrrolopyrimidine derivative and preparation method and application thereof
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Paragraph 0137-0138; 0141; 0151-0152, (2020/05/14)
The invention relates to a 4-aminopyrrolopyrimidine derivative and a preparation method and application thereof, and belongs to the field of medicines. The invention provides a compound shown as a formula I or pharmaceutically acceptable salt thereof. The
Synthesis and Pharmacological Evaluation of Noncatechol G Protein Biased and Unbiased Dopamine D1 Receptor Agonists
Wang, Pingyuan,Felsing, Daniel E.,Chen, Haiying,Raval, Sweta R.,Allen, John A.,Zhou, Jia
supporting information, p. 792 - 799 (2019/05/02)
Noncatechol heterocycles have recently been discovered as potent and selective G protein biased dopamine 1 receptor (D1R) agonists with superior pharmacokinetic properties. To determine the structure-activity relationships centered on G protein or β-arrestin signaling bias, systematic medicinal chemistry was employed around three aromatic pharmacophores of the lead compound 5 (PF2334), generating a series of new molecules that were evaluated at both D1R Gs-dependent cAMP signaling and β-arrestin recruitment in HEK293 cells. Here, we report the chemical synthesis, pharmacological evaluation, and molecular docking studies leading to the identification of two novel noncatechol D1R agonists that are a subnanomolar potent unbiased ligand 19 (PW0441) and a nanomolar potent complete G protein biased ligand 24 (PW0464), respectively. These novel D1R agonists provide important tools to study D1R activation and signaling bias in both health and disease.
CANCER TREATMENTS TARGETING CANCER STEM CELLS
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Paragraph 0331; 0337-0339, (2019/11/19)
Disclosed are compounds, methods, compositions, and kits that allow for treating cancer by, e.g., targeting cancer stem cells. In some embodiments, the cancer is colorectal cancer, gastric cancer, gastrointestinal stromal tumor, ovarian cancer, lung cancer, breast cancer, pancreatic cancer, prostate cancer, testicular cancer, or lymphoma. In some embodiments, the cancer is liver cancer, endometrial cancer, leukemia, or multiple myeloma. The compounds utilized in the disclosure are of Formula (0), (O'), and (I):
Identification of 5-(2,3-Dihydro-1 H-indol-5-yl)-7 H-pyrrolo[2,3- d]pyrimidin-4-amine Derivatives as a New Class of Receptor-Interacting Protein Kinase 1 (RIPK1) Inhibitors, Which Showed Potent Activity in a Tumor Metastasis Model
Li, Yueshan,Xiong, Yu,Zhang, Guo,Zhang, Liting,Yang, Wei,Yang, Jiao,Huang, Luyi,Qiao, Zeen,Miao, Zhuang,Lin, Guifeng,Sun, Qiu,Niu, Ting,Chen, Lijuan,Niu, Dawen,Li, Linli,Yang, Shengyong
, p. 11398 - 11414 (2019/01/08)
We herein report the structural optimization and structure-activity relationship studies of 5-(2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine derivatives as a new class of receptor-interacting protein kinase 1 (RIPK1) inhibitors. Among all obtained RIPK1 inhibitors, 1-(5-{4-amino-7-ethyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl}-2,3-dihydro-1H-indol-1-yl)-2-[3-(trifluoromethoxy)phenyl]ethan-1-one (22b) is the most active one. This compound potently inhibited RIPK1 with a binding affinity (KD) of 0.004 μM and an enzymatic IC50 value of 0.011 μM and also showed good kinase selectivity. It could efficiently protect cells from necroptosis and attenuate the necrotic cell death of vascular endothelial cells induced by tumor cells both in vitro and in vivo. Importantly, compound 22b exhibited excellent antimetastasis activity in the experimental B16 melanoma lung metastasis model. It also displayed favorable pharmacokinetic properties. Collectively, 22b could be a promising agent for preventing tumor metastasis.
4,5,6,7-TETRAHYDRO-1 H-PYRAZOLO[4,3-C]PYRIDIN-3-AMINE COMPOUNDS AS CBP AND/OR EP300 INHIBITORS
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Page/Page column 300, (2016/06/14)
The present invention relates to compounds of formula (I) or formula (II): and to salts thereof, wherein R1-R4 of formula (I) and R1-R3 of formula (II) have any of the values defined herein, and compositions and uses thereof. The compounds are useful as inhibitors of CBP and/or EP300. Also included are pharmaceutical compositions comprising a compound of formula (I) of formula (II) or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various CBP and/or EP300-mediated disorders.
HETEROCYCLIC CGRP RECEPTOR ANTAGONISTS
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Page/Page column 81, (2016/05/19)
The present invention is directed to heterocyclic compounds which are antagonists of CGRP receptors and may be useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
Pesticidal compositions and processes related thereto
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, (2016/01/09)
This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.
Discovery of a novel series of N-phenylindoline-5-sulfonamide derivatives as potent, selective, and orally bioavailable Acyl CoA:monoacylglycerol acyltransferase-2 inhibitors
Sato, Kenjiro,Takahagi, Hiroki,Yoshikawa, Takeshi,Morimoto, Shinji,Takai, Takafumi,Hidaka, Kousuke,Kamaura, Masahiro,Kubo, Osamu,Adachi, Ryutaro,Ishii, Tsuyoshi,Maki, Toshiyuki,Mochida, Taisuke,Takekawa, Shiro,Nakakariya, Masanori,Amano, Nobuyuki,Kitazaki, Tomoyuki
supporting information, p. 3892 - 3909 (2015/05/27)
Acyl CoA:monoacylglycerol acyltransferase-2 (MGAT2) has attracted interest as a novel target for the treatment of obesity and metabolic diseases. Starting from N-phenylbenzenesulfonamide derivative 1 with moderate potency for MGAT2 inhibition, we explored
INDOLINE DERIVATIVES AS INHIBITORS OF PERK
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Page/Page column 73; 74, (2015/05/05)
The invention is directed to substituted indoline derivatives. Specifically, the invention is directed to compounds according to Formula I: (I) wherein R1, R2 and R3 are defined herein. The compounds of the invention are inhibitors of PERK and can be usef