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Sulfur(vi) fluoride compounds and methods for the preparation thereof

A technology of compounds and substances, applied in the field of preparing said compounds and compositions

Active Publication Date: 2017-05-10
THE SCRIPPS RES INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Thus, despite its high-energy nature, this click reaction, triggered by finding a way to induce two functional groups to interact with each other, has only a very small possibility of reacting with any species.

Method used

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  • Sulfur(vi) fluoride compounds and methods for the preparation thereof
  • Sulfur(vi) fluoride compounds and methods for the preparation thereof
  • Sulfur(vi) fluoride compounds and methods for the preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment approach

[0248] According to one embodiment, the pharmaceutical combination of the present invention suitable for vaginal administration is provided in the form of a diaphragm, tampon, cream, gel, ointment, foam or sponge, which comprises the compound of formula (I) of the present invention. Compounds and carriers known in the art. Alternatively, compositions suitable for vaginal administration may be delivered in liquid or solid dosage form. Additives, excipients, etc. are generally included in compositions for vaginal administration in concentration ranges suitable for their intended use or function in the composition, as is known in the art of pharmaceutical formulation. The compounds of formula (I) are contained in the compositions in a therapeutically useful and effective concentration range as determined by routine methods known in the medical and pharmaceutical arts. For example, a typical composition may contain one or more compounds of formula (I) in a concentration ranging f...

example 1

[0295] Example 1 (A) for short.

[0296] BEMP=2-tert-butylimino-2-diethylamino-1,3-dimethylperhydro-1,3,2-diazaphosphine, DBN=1,5-diazabicyclo[4.3 .0]non-5-ene, DBU=1,8-diazabicyclo[5.4.0]undec-7-ene, LHMDS=bis(trimethylsilyl)amide lithium, TCEP=tri( 2-carboxyethyl)phosphine hydrochloride, TMS = trimethylsilyl, TBS = tert-butyldimethylsilyl chloride.

[0297] Example 1 (B) General method.

[0298] Recorded on Bruker DRX-500, Bruker DRX-600, Bruker AMX-400 instruments 1 H and 13 C NMR spectra, and chemical shifts (δ) expressed in parts per million, as residual CHCl 3 , acetone, acetonitrile or DMSO as internal standard. Proton Magnetic Resonance ( 1 (HNMR) spectra were recorded at 600, 500 or 400 MHz. carbon magnetic resonance ( 13 C NMR) spectra were recorded at 150, 125 or 101 MHz. Fluorine magnetic resonance ( 19 F NMR) spectra were recorded at 376 MHz. NMR acquisitions were performed at 295K unless otherwise stated. The abbreviations are: s, singlet; d, doublet;...

example 2

[0456] Example 2 Modified Antibiotics

[0457] ArOSO 2 F is a non-polar functional group on the aromatic ring. It is an electrophile capable of coexisting with nucleophiles and capable of sustaining biological systems. ArOSO 2 F is very stable and can selectively react with different protein targets. Its non-polar functionality means that the introduction of functional groups on the parent has minimal or no effect on the affinity of the parent molecule.

[0458] Any known small molecule drug with one or more aromatic substitutions can be easily converted to ArOSO 2 F. Many antibiotics include functional groups such as aryl-OH, amino groups, etc., which can be derivatized to introduce SO 2 F group (such as OSO 2 F. NCH 2 CH 2 SO 2 F or NSO 2F) into the antibiotic structure. In this study, five fluorosulfonyl antibiotic derivatives (cephalosporin derivative 10-2, ciprofloxacin derivative 10-7 and three vancomycin derivatives - vancomycin-SF, vancomycin Mymycin-SF-1 ...

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Abstract

This application describes a compound represented by Formula (I): (I) wherein: Y is a biologically active organic core group comprising one or more of an aryl group, a heteroaryl aryl group, a nonaromatic hydrocarbyl group, and a nonaromatic heterocyclic group, to which Z is covalently bonded; n is 1, 2, 3, 4 or 5; m is 1 or 2; Z is O, NR, or N; X1 is a covalent bond or -CH2CH2-, X2 is O or NR; and R comprises H or a substituted or unsubstituted group selected from an aryl group, a heteroaryl aryl group, a nonaromatic hydrocarbyl group, and a nonaromatic heterocyclic group. Methods of preparing the compounds, methods of using the compounds, and pharmaceutical compositions comprising the compounds are described as well.

Description

[0001] Cross-references to related applications [0002] This application claims priority to U.S. Provisional Patent Application No. 62 / 008,925, filed June 6, 2014, the entire contents of which are hereby incorporated by reference. [0003] governmental support [0004] This invention was made with government support from National Institutes of Health Grant Nos. U01NS058046 and EB015663 and National Science Foundation Grant No. CHE 1011796. The United States Government holds certain rights in this invention. Technical field [0005] The present invention relates to sulfur(VI) fluoride compounds, including therapeutic compounds and compositions, as well as methods of using the compounds and compositions and methods of making the compounds and compositions. Background technique [0006] More than a decade ago, "click" chemistry was introduced as a conceptual framework for the assembly of functional molecules, which emphasized the importance of carbon-heteroatom bonds in conn...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/10A61K31/16A61K38/095
CPCC07C305/26C07D277/82C07D295/088C07D295/185C07D295/26C07C2601/14C07C2603/18A61K47/54A61K31/05A61K31/136A61K31/14A61K31/197A61K31/198A61K31/397A61K31/40A61K31/4045A61K31/407A61K31/4168A61K31/4245A61K31/4353A61K31/439A61K31/47A61K31/4709A61K31/473A61K31/4745A61K31/485A61K31/505A61K31/515A61K31/53A61K31/5513A61K31/56A61K31/65A61K31/655A61K31/70A61K31/7048A61K38/31A61P21/00A61P21/02A61P25/04A61P25/08A61P25/20A61P25/24A61P29/00A61P31/00A61P31/04A61P43/00A61P5/24A61P5/38C07K7/16A61K51/0491A61K51/0406C07D279/08C07D501/18A61K51/0497C07K1/02C07K1/1136C07K2/00
Inventor 董佳佳K·B·沙普利斯J·W·凯利A·巴朗扎卡陈文涛
Owner THE SCRIPPS RES INST
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