- JAK Inhibitor with high oral bioavailability
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The JAK inhibitor has high oral bioavailability, and is characterized in that the JAK inhibitor comprises a compound of the formula I, or a stereoisomer thereof. A geometric isomer, a tautomer, a hydrate, a solvate, and a pharmaceutically acceptable salt
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Paragraph 0081-0082; 0085-0086
(2021/11/06)
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- Pharmaceutical compound used as JAK kinase inhibitor
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The invention provides a pharmaceutical compound. The pharmaceutical compound is a compound shown in the following structural formula or a stereoisomer, a geometrical isomer, a tautomer, a racemate, ahydrate, a solvate, a metabolite and a pharmaceutically acceptable salt or prodrug thereof shown in the specification, wherein R represents 1 to 3 substituents on a benzene ring, and each of the 1 to3 substituents is independently selected from halogen or cyano. The pharmaceutical compound provided by the invention can inhibit JAK kinase, and more particularly can be used as a JAK1/Tyk2 dual inhibitor and a Tyk2 specific inhibitor. More specifically, the pharmaceutical compound provided by the invention can be used for preventing or treating autoimmune diseases such as rheumatoid arthritis,ankylosing spondylitis, ulcerative colitis, systemic lupus erythematosus, type I diabetes, sicca syndrome, vasculitis, alopecia areata, psoriasis, leucoderma and the like, or other inflammatory skin diseases such as atopic dermatitis, eczema, acne and hidradenitis suppurativa.
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Paragraph 0056; 0060-0061
(2020/12/05)
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- HYDANTOIN CONTAINING DEOXYURIDINE TRIPHOSPHATASE INHIBITORS
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Provided herein are dUTPase inhibitors, compositions comprising such compounds and methods of using such compounds and compositions.
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- Acylated 4-amidino- and -4-guanidinobenzylamines for inhibition of plasma kallikrein
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The invention relates to the use of acylated 4-amidino- or 4-guanidinobenzylamine in accordance with the general formula I P4-P3-P2-P1??(I), where P4 is a monosubstituted or polysubstituted or unsubstituted benzylsulfonyl group, P3 is a monosubstituted or polysubstituted or unsubstituted, natural or unnatural α-amino acid or α-imino acid in the D configuration, P2 is a monosubstituted or polysubstituted or unsubstituted, natural or unnatural α-amino acid or α-imino acid in the L configuration, and P1 is a monosubstituted or polysubstituted or unsubstituted 4-amidino- or 4-guanidinobenzylamine group, for inhibiting plasma kallikrein (PK), factor XIa and factor XIIa, in particular for preventing the activation of coagulation at synthetic surfaces and for systemic administration as anticoagulants/antithrombotic agents, in particular for preventing the activation of coagulation at synthetic surfaces for the purpose of averting thromboembolic events.
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- Indole cytosolic phospholipase A2 α inhibitors: Discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4- dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl} benzoic acid, efipladib
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The optimization of a class of indole cPLA2α inhibitors is described herein. The importance of the substituent at C3 and the substitution pattern of the phenylmethane sulfonamide region are highlighted. Optimization of these regions led to the
- McKew, John C.,Lee, Katherine L.,Shen, Marina W. H.,Thakker, Paresh,Foley, Megan A.,Behnke, Mark L.,Hu, Baihua,Sum, Fuk-Wah,Tam, Steve,Hu, Yonghan,Chen, Lihren,Kirincich, Steven J.,Michalak, Ronald,Thomason, Jennifer,Ipek, Manus,Wu, Kun,Wooder, Lane,Ramarao, Manjunath K.,Murphy, Elizabeth A.,Goodwin, Debra G.,Albert, Leo,Xu, Xin,Donahue, Frances,Ku, M. Sherry,Keith, James,Nickerson-Nutter, Cheryl L.,Abraham, William M.,Williams, Cara,Hegen, Martin,Clark, James D.
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experimental part
p. 3388 - 3413
(2009/05/26)
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- Process for making an aldehyde
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A process for making an aromatic aldehyde in which a sulfoxide is reacted with a dihalogenated aromatic compound in the absence of an effective amount of an activating reagent. The aldehyde may then be used to make other compounds, such as a compound that acts as a cPLA inhibitor.
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