- COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH STING ACTIVITY
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This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt, and/or hydrate, and/or cocrystal, and/or drug combination of the compound) that inhibit (e.g., antagonize) Stimulator of Interferon Genes (STING). Said chemical entities are useful, e.g., for treating a condition, disease or disorder in which increased (e.g., excessive) STING activation (e.g., STING signaling) contributes to the pathology and/or symptoms and/or progression of the condition, disease or disorder (e.g., cancer) in a subject (e.g., a human). This disclosure also features compositions containing the same as well as methods of using and making the same.
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Page/Page column 178-179
(2020/07/31)
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- Nonenzymatic, enantioconvergent dynamic kinetic resolution (DKR) of racemic 2-(1H-pyrrol-1-yl)alkanoic acids as α-amino acid equivalents
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We report an effective dynamic kinetic resolution (DKR) system of racemic 2-(1H-pyrrol-1-yl)alkanoic acids, which consists of a rapid racemization step via an activating substrate and an enantio-discriminating step via catalytic esterification. The combination of pivalic anhydride as an activating agent, bis(α-naphthyl)methanol as an achiral alcohol, (R)-BTM as a chiral acyl-transfer catalyst, and Hunig's base converted racemic 2-(1H-pyrrol-1-yl)alkanoic acids to the corresponding chiral carboxylates, which can be transformed into chiral α-amino acid derivatives with maintained high enantiopurity.
- Tokumaru, Eri,Tengeiji, Atsushi,Nakahara, Takayoshi,Shiina, Isamu
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supporting information
p. 1768 - 1770
(2016/02/18)
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- Hetrocyclic systems containing azindole: Synthesis and pharmacological screening of 1-(H/bromo/chloro/nitro/methyl substituted phenyloxy)acetyl/propionyl>benzimidazoles
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Benzimidazole on treatment with α-chloroacetic or propionic acid gives benzimidazole-1-acetic or propionic acid (1a/1b) which on refluxing with thionyl chloride affords the corresponding chloride (2a/2b).The chlorides 2a,b react with bromo, chloro, nitro
- Halwe, Kirti,Srivastava, Santosh Kumar
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p. 710 - 713
(2007/10/02)
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