- Syntheses of PDE3A inhibitor ORG9935 and determination of the absolute stereochemistries of its enantiomers by X-ray crystallography
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Two synthetic methods were developed for the synthesis of PDE3A inhibitor ORG9935. The first one proceeds in six steps and 34% overall yield and the second one in five steps and an overall yield of 69% starting from commercially available starting materia
- Jakkaraj, Sudhakar R.,Young, Victor G.,Georg, Gunda I.
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- BENZOTHIOPHENE COMPOUND, PREPARATION METHOD THEREFOR AND USE THEREOF
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A compound represented by formula (I) or a pharmaceutically acceptable salt, a stereoisomer, a tautomer, a polymorph, a solvate, an N-oxide, an isotope labeled compound, a metabolite or a prodrug thereof, a pharmaceutical composition and a pill container comprising same, a preparation method therefor, and the use thereof in the preparation of drugs for preventing or treating STING-mediated related diseases.
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Paragraph 0183; 0186; 0187
(2022/03/22)
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- Benzothiophene compound or pharmaceutically acceptable salt and isomer thereof, and preparation method, pharmaceutical composition and application of benzothiophene compound or pharmaceutically acceptable salt and isomer thereof
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The invention discloses a benzothiophene compound with a structure as shown in a general formula I or a pharmaceutically acceptable salt, an isomer, a preparation method of the benzothiophene compound, a pharmaceutical composition and application of the benzothiophene compound. The invention overcomes the defects that the existing interferon gene stimulating protein micromolecule agonist is lack, the druggability of the nucleotide interferon gene stimulating protein agonist is poor and the like, has good agonistic activity on interferon gene stimulating protein, and has a good treatment effect on tumors and infectious diseases.
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- Amide compound and preparation method and application thereof
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The invention relates to an amide compound and a preparation method and application thereof. Specifically, the present invention relates to a compound of formula I or a pharmaceutically acceptable salt, stereoisomer, tautomer, polymorph, solvate, N-oxide, isotope labeled compound, metabolite or prodrug thereof, pharmaceutical compositions and kits comprising the same, processes for their preparation and their use in the preparation of medicaments for the treatment of STING-mediated related diseases.
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Paragraph 0200-0201; 0205-0207
(2020/11/12)
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- Benzothiophene amide compound and preparation method and application thereof
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The invention relates to a benzothiophene amide compound and a preparation method and application thereof. Specifically, the present application relates to a compound represented by formula (I), a stereoisomer, a tautomer, a polymorph, an N-oxide, an isotope labeled compound, a metabolite or a prodrug thereof, or a solvate or a pharmaceutically acceptable salt thereof, and the compound can be usedfor preparing a drug for treating a cell proliferative disease.
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Paragraph 0204-0205; 0209-0211
(2020/11/12)
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- Benzothiophene compound as well as pharmaceutical composition and application thereof
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The invention relates to a benzothiophene compound as well as a pharmaceutical composition and application thereof. Specifically, the compound disclosed by the invention has a structure shown as a formula I which is shown in the specification, and the definitions of all groups and substituents are as described in the specification. The invention also discloses a preparation method of the compoundand an application of the compound in tumor resistance.
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Paragraph 0141-0143
(2020/07/21)
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- BENZO[b]THIOPHENE COMPOUNDS AS STING AGONISTS
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Compounds of general formula (Ia), compounds of general formula (Ia′), compounds of general formula (Ib), compounds of general formula (Ib′), compounds of general formula (I), compounds of general formula (I′), and their pharmaceutically acceptable salts,
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Paragraph 0463; 0464
(2018/04/18)
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- Synthesis and agonistic activity at the GPR35 of 5,6-dihydroxyindole-2- carboxylic acid analogues
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5,6-Dihydroxyindole-2-carboxylic acid (DHICA), an intermediate of melanin synthesis and an eumelanin building block, was recently discovered to be a GPR35 agonist with moderate potency. Here, we report the synthesis and pharmacological characterization of a series of DHICA analogues against GPR35 using both label-free dynamic mass redistribution and Tango β-arrestin translocation assays. This led to identification of novel GPR35 agonists with improved potency and/or having biased agonism.
- Deng, Huayun,Fang, Ye
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p. 550 - 554
(2012/09/05)
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- FUSED RING ANALOGUES OF ANTI-FIBROTIC AGENTS
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The present invention relates to arylcarbonyl and heteroarylcarbonyl anthranilate compounds that may be useful as anti-fibrotic agents. The present invention also relates to methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment disorders.
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Page/Page column 97
(2011/05/06)
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- Benzothiophene derivatives
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This invention provides for pharmaceutical formulations of certain benzothiophene derivatives and a method of using the derivatives or formulations for the treatment of asthma.
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