173089-82-2Relevant articles and documents
TARGETED RADIOPHARMACEUTICALS FOR THE DIAGNOSIS AND TREATMENT OF PROSTATE CANCER
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Page/Page column 392, (2021/01/29)
A compound of general formula (I): wherein: n is 1, 2 or 3; R1, R2, R3 and R4, independently represent OH or Q; and 20 Q represents a tissue-targeting moeity selected from the group consisting of or a stereoisomer, a hydrate, a solvate, or a salt thereof, or a mixture of same, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said 25 compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of soft tissue diseases, as a sole agent or in combination with other active ingredients.
BICYCLIC COMPOUNDS
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Paragraph 00254, (2020/06/01)
Provided herein are compounds and pharmaceutical compositions comprising said compounds that are useful for treating cancers. Specific cancers include those that are mediated by YAP/TAZ or those that are modulated by the interaction between YAP/TAZ and TEAD.
Discovery of 2-substituted-N-(3-(3,4-dihydroisoquinolin-2(1H)-yl)-2-hydroxypropyl)-1,2,3,4-tetrahydroisoquinoline-6-carboxamide as potent and selective protein arginine methyltransferases 5 inhibitors: Design, synthesis and biological evaluation
Shao, Jingwei,Zhu, Kongkai,Du, Daohai,Zhang, Yuanyuan,Tao, Hongrui,Chen, Zhifeng,Jiang, Hualiang,Chen, Kaixian,Luo, Cheng,Duan, Wenhu
, p. 317 - 333 (2019/01/04)
Protein arginine methyltransferases 5 (PRMT5) represents an attractive drug target in epigenetic field for the treatment of leukemia and lymphoma. Here, a series of N-(3-(3,4-dihydroisoquinolin-2(1H)-yl)-2-hydroxypropyl)amide derivatives targeting PRMT5 were designed with structure-based approach and synthesized. Among them, compound 46 showed potent and selective PRMT5 inhibition activity with an IC50 of 8.5 nM, which was approximately equivalent with the phase I clinical trial PRMT5 inhibitor GSK-3326595 (IC50 = 5.5 nM). Compound 46 also displayed pronounced anti-proliferative activity in MV4-11 cells (GI50 = 18 nM) and antitumor activity in MV4-11 mouse xenografts model. This molecule can serve as an excellent tool compound for probing the biological function of PRMT5.
Azacyclic derivative as well as preparation method and medical use thereof
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, (2019/02/04)
The invention relates to an azacyclic derivative as well as a preparation method and medical use thereof and particularly relates to an azacyclic derivative represented by a general formula (I) (shownin the description), a preparation method thereof, a pharmaceutical composition containing the derivative and use of the derivative as an SMO antagonist, particularly in the treatment of diseases such as cancer related to Hedgehog signal channels. The definitions of groups in the general formula (I) are same as the definitions in the description.
CONDENSED RING DERIVATIVE, AND PREPARATION METHOD, INTERMEDIATE, PHARMACEUTICAL COMPOSITION AND USE THEREOF
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Paragraph 0187; 0188, (2018/02/28)
Disclosed are a condensed ring derivative, and a preparation method, an intermediate, a pharmaceutical composition and a use thereof. The condensed ring derivative of the present invention has a significant inhibitive effect on URAT1, which can effectively alleviate or treat hyperuricemia and other related diseases.
Imidazole-containing condensed tricyclic compound and application thereof
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Paragraph 0363; 0369, (2018/03/01)
The invention discloses an imidazole-containing condensed tricyclic compound adopting the structure as shown in the formula (I) or pharmaceutically acceptable salts, stereisomers or prodrug molecules thereof. The imidazole-containing condensed tricyclic compound has the IDO1 activity regulation function, can enhance T-cell activation through blocking immune checkpoints IDO1, is used for treating IDO1-mediated immunosuppression, and therefore, can become an effective medicine for treating malignant tumors. When used together with checkpoint protein anti-body drugs or other anti-cancer drugs, the imidazole-containing condensed tricyclic compound can enhance the anti-cancer effect. Meanwhile, the imidazole-containing condensed tricyclic compound has the potential of effectively treating IDO1 abnormity related immunosuppressive diseases and has a high application value.
Preparation method of 1-aminoisoquinoline-6-methanol
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, (2017/08/29)
The invention relates to a synthesis method of 1-aminoisoquinoline-6-methanol. The synthesis method comprises the following steps: reacting 6-bromoisoquinoline used as a raw material to form 6-cyanoisoquinoline; adding a sulfuric acid solution to obtain isoquinoline-6-carboxylic acid; further obtaining isoquinoline-6-methyl formate under the action of absolute methanol and thionyl chloride; further adding m-chloroperoxybenzoic acid in batches in dichloromethane, and reacting to obtain a mixture isoquinoline-6-methyl formate oxynitride; adding into phosphorus oxychloride in batches, cooling after the reaction is completed, pouring into cracked ice, and precipitating a solid 1-chloroisoquinoline-6-methyl formate crude product; directly extracting the water phase with ethyl acetate, and performing centrifugal drying to obtain another 1-chloroisoquinoline-6-methyl formate crude product; merging the crude products of two batches, passing through a silica gel column, and eluting to obtain 1-chloroisoquinoline-6-methyl formate; adding into tetrahydrofuran, then cooling to -30 DEG C, and adding lithium aluminum hydride in batches to obtain a 1-(1-chloroisoquinoline-6-yl)methanol product; mixing with p-methoxybenzylamine, and heating to obtain (1-(4-methoxybenzylamino)isoquinoline-6-yl)methanol; and adding into trifluoroacetic acid, and refluxing to obtain the final product 1-aminoisoquinoline-6-methanol. The method is reasonable in route, low in waste, high in yield and easy to operate, and realizes raw material saving.
PYRROLOPYRIMIDINE COMPOUNDS USED AS TLR7 AGONIST
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Paragraph 0117, (2017/07/29)
The present invention relates to a pyrrolopyrimidine compound as TLR7 agonist, and particularly relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof, a preparation process thereof, a pharmaceutical composition containing such compounds and use thereof for manufacturing a medicament against viral infection.
Pyrrolo pyrimidine ring compound, its use and pharmaceutical composition (by machine translation)
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Page/Page column 61; 62, (2017/07/31)
The invention relates to an as TLR7 agonist of the pyrrolo pyrimidine compounds, specifically on a compound of formula (I) compound or its pharmaceutically acceptable salt, preparation method thereof, containing the compounds of the pharmaceutical composition, and its use for the preparation of antiviral drug use. Formula (I) (by machine translation)
HETEROCYCLIC MODULATORS OF PKB
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Page/Page column 106-107, (2009/03/07)
The invention relates to heterocyclic compounds of Formula I and compositions thereof useful for treating diseases mediated by protein kinase B (PKB) where the variables have the definitions provided herein Formula (I). The invention also relates to the therapeutic use of such compounds and compositions thereof in treating disease states associated with abnormal cell growth, cancer, inflammation, and metabolic disorders.
