Patent classifications
C07C309/35
SALT OF QUINAZOLINE DERIVATIVE, PREPARATION METHOD THEREFOR AND APPLICATION THEREOF
A salt of a quinazoline derivative (N-[4-(3-chlorine-4-fluoanilino)]-7-(3-morpholinepropanol)-6-(2-fluoroacrylamide)-quinazoline, the structure thereof is as represented by formula I). Compared with a known quinazoline derivative, the salt of the quinazoline derivative has one or more improved properties and at least has better water solubility, wherein a citrate, a benzene sulfonate, and an ethanedisulphonate thereof further have better crystallinity and are not easy to absorb moisture.
##STR00001##
SALT OF QUINAZOLINE DERIVATIVE, PREPARATION METHOD THEREFOR AND APPLICATION THEREOF
A salt of a quinazoline derivative (N-[4-(3-chlorine-4-fluoanilino)]-7-(3-morpholinepropanol)-6-(2-fluoroacrylamide)-quinazoline, the structure thereof is as represented by formula I). Compared with a known quinazoline derivative, the salt of the quinazoline derivative has one or more improved properties and at least has better water solubility, wherein a citrate, a benzene sulfonate, and an ethanedisulphonate thereof further have better crystallinity and are not easy to absorb moisture.
##STR00001##
PSILOCIN MUCATE
Psilocin formulations of psilocin mucate with improved stability, physical properties and/or handling characteristics, as well as enhanced pharmacologic activity, pharmacokinetic parameters and safety characteristics as compared to psilocin or psilocybin and methods for their use are provided.
FORMULATIONS OF A MACROCYCLIC TRK KINASE INHIBITOR
The present application in some embodiments provides a pharmaceutical composition comprising:
##STR00001## and a compounding agent. Further provided herein are methods of making and methods of using the pharmaceutical compositions, for example, in the treatment of cancer.
Coating Composition Comprising Compound, And Organic Light Emitting Device Comprising Same
The present specification relates to a coating composition comprising a compound, and an organic light emitting device comprising the same.
SALTS AND CRYSTAL FORMS OF OMECAMTIV MECARBIL
Provided herein are free base crystalline forms, crystalline salts, and an amorphous salts of omecamtiv mecarbil.
SALTS OF AN EPIDERMAL GROWTH FACTOR RECEPTOR KINASE INHIBITOR
The present invention provides a salt form and compositions thereof, which are useful as an inhibitor of EGFR kinases and which exhibits desirable characteristics for the same.
SALTS OF AN EPIDERMAL GROWTH FACTOR RECEPTOR KINASE INHIBITOR
The present invention provides a salt form and compositions thereof, which are useful as an inhibitor of EGFR kinases and which exhibits desirable characteristics for the same.
PHENOTHIAZINE DIAMINIUM SALTS AND THEIR USE
- Colin Marshall ,
- Scott Clunas ,
- John Mervyn David Storey ,
- James Peter Sinclair ,
- Thomas Craven Baddeley ,
- Ahtsham Ishaq ,
- Michael Simpson ,
- Craig Williamson ,
- Barry Alan Wood ,
- Claude Michel Wischik ,
- Charles Robert Harrington ,
- Janet Elizabeth Rickard ,
- David Horsley ,
- Yin Sze Loh ,
- Karrar Ahmad Khan ,
- Christopher Paul Larch
Disclosed are compounds of general formula (I):
##STR00001##
and pharmaceutically acceptable salts thereof, formulations, methods and uses in, for example, the treatment of disease.
SALTS OF MORPHOLINE DERIVATIVE, CRYSTAL FORMS THEREOF, PROCESSES FOR PRODUCING THE SAME, PHARMACEUTICAL COMPOSITIONS INCLUDING THE SAME, AND USE THEREOF
The present invention provides novel pharmaceutically acceptable salts of a morpholine derivative, including a malate, a tartrate, a hydrochloride, an acetate, and a naphthalene disulfonate thereof, wherein the tartrate has 3 crystal salt forms: crystal form A, crystal form B and dihydrate; the malate, the hydrochloride, and the acetate each have one crystal salt form; the naphthalene disulfonate is amorphous. When compared to the known morpholine derivative free base, the present invention has one or more improved properties, e.g., a better crystalline state, greatly improved water solubility, light stability and thermal stability, etc. The present invention further provides preparation methods for the salts of morpholine derivative and the crystal forms thereof, pharmaceutical compositions and use thereof.