- Glucuronide prodrugs of hydroxy compounds for antibody directed enzyme prodrug therapy (adept): A phenol nitrogen mustard carbamate
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A prodrug consisting of a β-D-glucuronic acid linked to a self-immolative spacer (a N-(ortho-hydroxyphenyl)-N-methylcarbamate) and a phenolic nitrogen mustard was synthesised. As this prodrug was easily cleaved by a β-glucuronidase enzyme and displayed lo
- Schmidt,Florent,Monneret,Straub,Czech,Gerken,Bosslet
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- BENZODICYCLOALKANE DERIVATIVE, PREPARATION METHOD AND USE THEREOF
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It is provided herein a benzobicycloalkane derivative, and a preparation method and use thereof. In particular, it is provided herein a compound of Formula (I), or a pharmaceutically acceptable salt, stereoisomer or solvate thereof, a preparation method, and a use thereof in preparation of drugs for treating pain.
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Paragraph 0154; 0348; 0349
(2019/06/19)
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- GLUCURONIDE PRODRUGS OF TOFACITINIB
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The invention relates to glucuronide prodrug compounds of the Janus kinase (JAK) inhibitor tofacitinib having formula (I): (Formula (I)) where A1 and R1 are as defined. The invention also relates to pharmaceutical compositions comprising such compounds; methods of using such compounds to treat gastrointestinal inflammatory diseases; and processes and intermediates for preparing such compounds.
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Page/Page column 44; 45
(2018/09/28)
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- GLUCURONIDE PRODRUGS OF JANUS KINASE INHIBITORS
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The invention relates to glucuronide prodrug compounds of Janus kinase (JAK) inhibitors having formula I: where W1, R1 and A1 are as defined. The invention also relates to pharmaceutical compositions comprising such compounds; methods of using such compounds to treat gastrointestinal inflammatory diseases; and processes and intermediates for preparing such compounds.
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Paragraph 0299; 0301; 0302
(2018/12/11)
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- Prodrugs for the therapy of tumors and inflammatory disorders
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Compounds of the formula Iglycosyl-Y[--C( Y)--X--] p --W(R) n --Z--C( Y)-active compound (I)are described which are suitable for the treatment of carcinomatous diseases, autoimmune diseases and chronic inflammatory diseases such as rheumatoid arthritis.
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