Patent classifications
C07C309/35
Method for the production of lumateperone and its salts
Method for the production of formula (I) lumateperone or its acid addition salts so that the enantiomer compound with stereochemistry 6bR,10aS ##STR00001##
is separated form the cis racemate using resolution and the formula (II) stereoisomer is alkylated with 4-halo-4′-fluoro butyrophenone (X=I, Br, Cl) to produce the formula (I) lumateperone, or optionally its acid addition salt. The object of the invention also relates to the amorphous form of the morphologically uniform p-toluenesulfonic acid salt of lumateperone and to the naphthalene-2-sulfonic acid salt of lumateperone, to the 1:2 stoichiometry salt of lumateperone formed with naphthalene-2-sulfonic acid.
PROCESSES OF MAKING AND CRYSTALLINE FORMS OF A MDM2 INHIBITOR
The present invention provides processes for making 2-((3R,5R,6S)-5-(3-chlorophenyl)-6-(4-chlorophenyl)-1-((S)-1-(isopropylsulfonyl)-3-methylbutan-2-yl)-3-methyl-2-oxopiperidin-3-yl)acetic acid as well as intermediates and processes for making the intermediates. Also provided are crystalline forms of the compound and the intermediates.
PROCESSES OF MAKING AND CRYSTALLINE FORMS OF A MDM2 INHIBITOR
The present invention provides processes for making 2-((3R,5R,6S)-5-(3-chlorophenyl)-6-(4-chlorophenyl)-1-((S)-1-(isopropylsulfonyl)-3-methylbutan-2-yl)-3-methyl-2-oxopiperidin-3-yl)acetic acid as well as intermediates and processes for making the intermediates. Also provided are crystalline forms of the compound and the intermediates.
A PRESERVATIVE COMPOSITION
The present invention provides a preservative composition to prevent and/or reduce corrosion on a metal surface comprising an anhydride-derived amide and an oil and/or a solvent, wherein the anhydride-derived amide is present in an amount in the range of from 0.01-50 wt %, based on the total weight of the preservative composition. The invention also provides a preservative composition comprising in addition a sulfonate composition; a metal article having a coating thereon which coating comprises the present preservative composition; and the use of the present preservative composition to prevent and/or reduce corrosion on a metal surface.
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.
ENANTIOMERICALLY PURIFIED GPER AGONIST FOR USE IN TREATING DISEASE STATES AND CONDITIONS
The present disclosure provides 1) an enantiomerically purified compound SRR G-1, or a derivative thereof, including specific crystal forms, salts and co-crystals that modulates G protein-coupled estrogen receptor activity, 2) pharmaceutical and cosmetic compositions comprising an enantiomerically purified SRR G-1, or a derivative thereof, and 3) methods of treating or preventing disease states and conditions and cosmetic conditions mediated through these receptors and related methods thereof in humans and animals.
SALTS AND CRYSTAL FORMS OF OMECAMTIV MECARBIL
Provided herein are free base crystalline forms, crystalline salts, and an amorphous salts of omecamtiv mecarbil.
Weakly coloured sulfonic acid
The subject of the present invention is a weakly corrosive and weakly coloured sulfonic acid, with an APHA colour index of less than 20, comprising chlorides and nitrites in a chloride/sulfonic acid molar ratio of between 1 ppm and 200 ppm, and a nitrite/sulfonic acid molar ratio of between 200 ppm and 6000 ppm, limits inclusive.