C07D203/08

Water-soluble propofol derivatives and uses thereof

The present invention discloses a class of water-soluble propofol derivatives, preparation method thereof, anesthetization method using the same, use thereof as prodrugs and use thereof in the preparation of intravenous anesthetics. The water-soluble propofol derivatives have the general formula (I); wherein X is H or F, Y is F or alkyl substituted by one or more F, n is 1, 2, 3, 4, 5 or 6, W is W.sup.1 or W.sup.2; W.sup.1 is NR.sup.1R.sup.2.A or ##STR00001##
R.sup.1 and R.sup.2 are each independently H, alkyl optionally substituted with phenyl, or cycloalkyl, m is 0, 1, 2 or 3, A is a pharmaceutically acceptable acid, W.sup.2 is COOM.sub.1/t or OPO.sub.3(M).sub.2/t or PO.sub.3(M).sub.2/t; M is a metal ion, an ammonium ion or a basic amino acid cation which can form a salt with an acid radical; t is the charge number of M. ##STR00002##

Water-soluble propofol derivatives and uses thereof

The present invention discloses a class of water-soluble propofol derivatives, preparation method thereof, anesthetization method using the same, use thereof as prodrugs and use thereof in the preparation of intravenous anesthetics. The water-soluble propofol derivatives have the general formula (I); wherein X is H or F, Y is F or alkyl substituted by one or more F, n is 1, 2, 3, 4, 5 or 6, W is W.sup.1 or W.sup.2; W.sup.1 is NR.sup.1R.sup.2.A or ##STR00001##
R.sup.1 and R.sup.2 are each independently H, alkyl optionally substituted with phenyl, or cycloalkyl, m is 0, 1, 2 or 3, A is a pharmaceutically acceptable acid, W.sup.2 is COOM.sub.1/t or OPO.sub.3(M).sub.2/t or PO.sub.3(M).sub.2/t; M is a metal ion, an ammonium ion or a basic amino acid cation which can form a salt with an acid radical; t is the charge number of M. ##STR00002##

Primecoat compositions for proteinaceous substrates and methods of priming proteinaceous substrates therewith
09636287 · 2017-05-02 · ·

Compositions containing a solution of a polyfunctional aziridine component in a non-reactive solvent, and methods of applying such compositions to proteinaceous substrates, such as fingernails and toenails, to provide primed substrates which may be further coated.

Primecoat compositions for proteinaceous substrates and methods of priming proteinaceous substrates therewith
09636287 · 2017-05-02 · ·

Compositions containing a solution of a polyfunctional aziridine component in a non-reactive solvent, and methods of applying such compositions to proteinaceous substrates, such as fingernails and toenails, to provide primed substrates which may be further coated.

COMPOSITIONS AND METHODS FOR TREATMENT OF INFLAMMATORY DISEASES OF THE LUNG
20170095445 · 2017-04-06 ·

Methods are for treatment of an inflammatory disease of the lung caused by inhalation of a toxic agent or an irritant, such as chlorine inhalational lung injury. The methods include administration of compositions including certain compounds.

CARBOXYLIC ACID DERIVATIVES AND USE THEREOF IN THE PREPARATION OF PRODRUGS

The present invention discloses a class of carboxylic acid derivatives and use thereof in preparation of prodrugs. The carboxylic acid derivatives have the general formula (I), wherein R.sup.1 is H or alkyl; X is H or F; Y is F or fluoroalkyl; n is 0, 1, 2, 3, 4, 5, or 6; W is W.sup.1 or W.sup.2; W.sup.1 is NR.sup.2R.sup.3, NR.sup.2R.sup.3.A,

##STR00001##

R.sup.2 and R.sup.3 are each independently H, alkyl, cycloalkyl, or a protecting group for amino; m is 0, 1, 2, or 3; A is an acid; W.sup.2 is COOR.sup.4, OPO(OR.sup.4).sub.2, or PO(OR.sup.4).sub.2; R.sup.4 is H, or a protecting group for carboxyl or hydroxyl in phosphoric acid.

##STR00002##

WATER-SOLUBLE PROPOFOL DERIVATIVES AND USES THEREOF

The present invention discloses a class of water-soluble propofol derivatives, preparation method thereof, anesthetization method using the same, use thereof as prodrugs and use thereof in the preparation of intravenous anesthetics. The water-soluble propofol derivatives have the general formula (I); wherein X is H or F, Y is F or alkyl substituted by one or more F, n is 1, 2, 3, 4, 5 or 6, W is W.sup.1 or W.sup.2; W.sup.1 is NR.sup.1R.sup.2.A or

##STR00001##

R.sup.1 and R.sup.2 are each independently H, alkyl optionally substituted with phenyl, or cycloalkyl, m is 0, 1, 2 or 3, A is a pharmaceutically acceptable acid, W.sup.2 is COOM.sub.1/t or OPO.sub.3(M).sub.2/t or PO.sub.3(M).sub.2/t; M is a metal ion, an ammonium ion or a basic amino acid cation which can form a salt with an acid radical; t is the charge number of M.

##STR00002##

WATER-SOLUBLE PROPOFOL DERIVATIVES AND USES THEREOF

The present invention discloses a class of water-soluble propofol derivatives, preparation method thereof, anesthetization method using the same, use thereof as prodrugs and use thereof in the preparation of intravenous anesthetics. The water-soluble propofol derivatives have the general formula (I); wherein X is H or F, Y is F or alkyl substituted by one or more F, n is 1, 2, 3, 4, 5 or 6, W is W.sup.1 or W.sup.2; W.sup.1 is NR.sup.1R.sup.2.A or

##STR00001##

R.sup.1 and R.sup.2 are each independently H, alkyl optionally substituted with phenyl, or cycloalkyl, m is 0, 1, 2 or 3, A is a pharmaceutically acceptable acid, W.sup.2 is COOM.sub.1/t or OPO.sub.3(M).sub.2/t or PO.sub.3(M).sub.2/t; M is a metal ion, an ammonium ion or a basic amino acid cation which can form a salt with an acid radical; t is the charge number of M.

##STR00002##

SYNTHESIS OF RAS INHIBITORS

The present invention relates to Ras inhibitors, intermediates in the synthesis thereto, and methods for preparing the Ras inhibitors and the intermediates.

SYNTHESIS OF RAS INHIBITORS

The present invention relates to Ras inhibitors, intermediates in the synthesis thereto, and methods for preparing the Ras inhibitors and the intermediates.