- [...] piperidine derivative and its preparation method and use thereof (by machine translation)
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The present invention provides a novel structure sila piperidine derivative or a pharmaceutically acceptable salt or solvate thereof, wherein the structure general formula is represented by a formula (I). The present invention further provides a drug composition containing a pharmaceutically effective amount of the sila piperidine derivative or the pharmaceutically acceptable salt or solvate thereof, and a pharmaceutically acceptable excipient or additive. The present invention further discloses a synthesis method for the sila piperidine derivative, wherein dichloro-substituted silane is adopted as a starting raw material, and multi-step reactions are integrated and performed in one pot to obtain the high purity pharmaceutical intermediate for preparing the camptothecin sila derivative, wherein the synthesis route is short, the reaction environments, especially the temperature, the pressure and the like, are safe and controlled, and the characteristic of green environmental protection is provided. In addition, the preparation raw materials have the wide sources and are easy to obtain, the preparation method is simple and is easy to operate, the reaction conditions are mild, the synthesized product yield is high, and great industrial application values are provided.
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Paragraph 0210; 0211; 0215-0216
(2018/08/28)
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- Design, Synthesis, and Identification of Silicon Incorporated Oxazolidinone Antibiotics with Improved Brain Exposure
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Therapeutic options for brain infections caused by pathogens with a reduced sensitivity to drugs are limited. Recent reports on the potential use of linezolid in treating brain infections prompted us to design novel compounds around this scaffold. Herein, we describe the design and synthesis of various oxazolidinone antibiotics with the incorporation of silicon. Our findings in preclinical species suggest that silicon incorporation is highly useful in improving brain exposures. Interestingly, three compounds from this series demonstrated up to a 30-fold higher brain/plasma ratio when compared to linezolid thereby indicating their therapeutic potential in brain associated disorders.
- Seetharamsingh,Ramesh, Remya,Dange, Santoshkumar S.,Khairnar, Pankaj V.,Singhal, Smita,Upadhyay, Dilip,Veeraraghavan, Sridhar,Viswanadha, Srikant,Vakkalanka, Swaroop,Reddy, D. Srinivasa
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supporting information
p. 1105 - 1110
(2015/11/24)
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- SILA ANALOGS OF OXAZOLIDINONE DERIVATIVES AND SYNTHESIS THEREOF
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The invention discloses silaanalogs of oxazolidinone compounds, to pharmaceutical compositions and to the synthesis of the oxazolidinone derivatives of formula I. The invention further relates to methods of treating a subject suffering with gram positive pathogens including those resistant to methicillin and vancomycin using the compound(s) or modulation of coagulation properties of blood-clotting cascade or compositions of the oxazolidinone derivatives of the invention.
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Paragraph 0086
(2014/10/16)
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- SILA ANALOGS OF OXAZOLIDINONE DERIVATIVES AND SYNTHESIS THEREOF
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The invention discloses silaanalogs of oxazolidinone compounds, to pharmaceutical compositions and to the synthesis of the oxazolidinone derivatives of formula I. The invention further relates to methods of treating a subject suffering with gram positive pathogens including those resistant to methicillin and vancomycin using the compound(s) or modulation of coagulation properties of blood-clotting cascade or compositions of the oxazolidinone derivatives of the invention.
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Page/Page column 21
(2013/04/25)
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- NOVEL TRIAZOLOPYRIMIDINE DERIVATIVES
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The present invention relates to novel triazolopyrimidine derivatives of formula (I) as active ingredients which have microbiocidal activity, in particular fungicidal activity: wherein the substituents are as defined in claim 1.
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Page/Page column 15
(2008/06/13)
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- 4,4-dimethyl-1,4-thiasilinane and its S-functional derivatives
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Synthetic approaches to 4,4-dimethyl-1,4-thiasilinane and its S-functional derivatives, 4,4-dimethyl-1,4-thiasilinane S-oxide, 4,4-dimethyl-1,4-thiasilinane S,S-dioxide, 4,4-dimethyl- 1-(phenylsulfonylimino)-1,4-thiasilinane, and 1,4,4-trimethyl-1,4-thiasilinan-1-ylium iodide, were studied. The S-functional derivatives of 4,4-dimethyl-4-thiasilinane, unlike 3,3-dimethyl-3-thiasilinane, are hydrolytically stable.
- Suslova,Albanov,Shainyan
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p. 1234 - 1242
(2008/02/03)
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- Agent for the regulation of plant growth
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The present invention relates to new compositions and methods for the regulation of plant growth, especially for fruit abscission, acceleration of ripening and latex discharge of rubber trees, and to new active substances of the class of β-halogenoethylsilanes. The new active substances in the new composition corresponding to the formula STR1 wherein X is chlorine or bromine, A represents a radical --SR1, --NR2 R3, --OR4, --CH=CH2 or --CH2 --CH2 --X, B and C each independently represent --CH3, --CH=CH2 or --CH2 --CH2 --X, the symbols R1, R3 and R4 representing substituted or unsubstituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, phenyl or benzyl radicals, R2 denoting hydrogen or the same as R3, whereby R2 and R3 together with the adjacent nitrogen atom can also form a saturated or unsaturated ring system, and R4 can furthermore represent the group --COR5, whereby R5 stands for alkyl, alkenyl, alkynyl, halogenoalk(en)yl, substituted or unsubstituted phenylalk(en)yl, alkoxyalkyl, alkoxycarbonylalkyl, benzoylalkyl, cycloalkylalkyl, for substituted or unsubstituted phenyl or for a 5- or 6-membered heterocyclic radical.
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