Extended knowledge of Thiomorpholine 1,1-dioxide

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An Overview of Recent Advances in the Applications of Click Chemistry in the Synthesis of Bioconjugates with Anticancer Activities

The click chemistry is one of the most powerful C?N bond forming-reactions towards five-membered heterocycles. The copper-catalyzed azide-alkyne cycloaddition (CuAAC) has widely used in the discovery of anti-cancer drugs and many articles have been published in this field. This review article aims to review general mechanism aspects and the recent advances (2016?2019) of click chemistry for cancer therapy.

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Thiomorpholine – Wikipedia,
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Synthetic method JAKAK1 inhibitor Filgogogotinib (by machine translation)

The invention provides Filgogogotinib, which comprises the following steps: (1) reacting 2 – amino -6 -bromopyridine with p-methylbenzene derivatives, and preparing compound 1; (2) reacting compound 1 with hydroxylamine hydrochloride, N, N – diisopropylethylamine to obtain compound 2; (3) reacting compound 2 with thiomorpholine 3, 4 dioxides, thereby obtaining Filgogogotinib.) . compound (3) and compound (4) are reacted, yielding compound 5, compound [4], and azodiisobutyronitrile to react, and the compound 5; (6 1 -) 5 is reacted with the azodiisobutyronitrile -1. The route of synthesizing Filgogogou is firstly coupled and then closed loop, the raw material is cheap, the reaction operation is simple, the product is easy to purify, the yield is high, and the method is suitable for commercial scale production. (by machine translation)

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Thiomorpholine – Wikipedia,
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COMPOUNDS AND COMPOSITIONS AS SYK KINASE INHIBITORS

Provided here in area novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated Syk kinase activity

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CHEMOKINE CXCR4 RECEPTOR MODULATORS AND USES RELATED THERETO

The disclosure relates to chemokine CXCR4 receptor modulators and uses related thereto. The receptor modulators can be formulated to form pharmaceutical compositions comprising the disclosed compounds or pharmaceutically acceptable salts or prodrugs thereof. The compositions may be used for managing CXCR4 related conditions, typically prevention or treatment of viral infections abnormal cellular proliferation, retinal degeneration, inflammatory diseases, or as an immunostimulant or immunosuppressant or for managing cancer and may be administered with another active ingredient such as an antiviral agent or chemotherapeutic agent.

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CATHEPSIN CYSTEINE PROTEASE INHIBITORS

This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.

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Thiomorpholine – Wikipedia,
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SUBSTITUTED PYRAZOLO[3,4-b]PYRIDIN-6-CARBOXYLIC ACIDS AND METHOD OF USE

The present invention provides for compounds of formula (I) wherein R1, R2, R3, and R4 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions mediated and modulated by CFTR, including cystic fibrosis, Sjoegren’s syndrome, pancreatic insufficiency, chronic obstructive lung disease, and chronic obstructive airway disease. Also provided are pharmaceutical compositions comprised of one or more compounds of formula (I).

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C-3 NOVEL TRITERPENONE WITH C-17 REVERSE AMIDE DERIVATIVES AS HIV INHIBITORS

The present invention relates to C-3 novel triterpenone with C-17 reverse amide compounds of Formula (I); and pharmaceutically acceptable salts thereof, wherein ring Formula (II), R1, R2, R3, R4, R5, R6, R7, ‘n’ and ‘m’ are as defined in Formula (I). The invention also relates to C-3 novel triterpenone with C-17 reverse amide derivatives, related compounds, and pharmaceutical compositions useful for the therapeutic treatment of viral diseases and particularly HIV mediated diseases.

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PYRROLOPYRIDINEAMINO DERIVATIVES AS MPS1 INHIBITORS

The present invention relates to the use of certain pyrrolopyridineamino derivatives (hereinafter referred to as “PPA derivatives”), particularly 1H-pyrrolo[3,2-c]pyridine-6-amino derivatives, to inhibit the spindle checkpoint function of Monospindle 1 (Mpsl also known as TTK) kinases either directly or indirectly via interaction with the Mps kinase itself. In particular, the present invention relates to PPA derivatives for use as therapeutic agents for the treatment and/or prevention of proliferative diseases, such as cancer. The present invention also relates to processes for the preparation of the PPA derivatives, and pharmaceutical compositions comprising them. Formula (1)

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HETEROCYCLIC COMPOUND

The present invention provide a heterocyclic compound having a HDAC inhibitory action, and useful for the treatment of autoimmune diseases and/or inflammatory diseases, graft versus host disease, cancers, central nervous diseases including neurodegenerative diseases, Charcot-Marie-Tooth disease and the like, and a pharmaceutical composition comprising the compound. The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.

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Inhibiting SSAO/VAP – 1 of amine compounds and their use in medicine (by machine translation)

The invention relates to a method for inhibiting semicarbazide-sensitive oxidase (SSAO) and/or vascular adhesion protein – 1 (VAP – 1) inhibitors of amine compounds and their use in medicine, further relates to the pharmaceutical composition. Said compound of the invention and pharmaceutical composition can be used for treating inflammation and/or inflammation-related diseases, diabetes and/or diabetes-related diseases, psychiatric disorders, ischemic disease, vascular disease, fibrosis or tissue transplant rejection. (by machine translation)

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem