Patent classifications
C07C215/60
LIGANDS FOR IMAGING CARDIAC INNERVATION
Novel compounds that find use as imaging agents within nuclear medicine applications (PET imaging) for imaging of cardiac innervation are disclosed. These PET based radiotracers may exhibit increased stability, decreased NE release (thereby reducing side effects), improved quantitative data, and/or high affinity for VMAT over prior radiotracers. Methods of using the compounds to image cardiac innervation are also provided. In some instances the compounds are developed by derivatizing certain compounds with 18F in a variety of positions: aryl, alkyl, a keto, benzylic, beta-alkylethers, gamma-propylalkylethers and beta-proplylalkylethers. Alternatively or additionally, a methyl group a is added to the amine, and/or the catechol functionality is either eliminated or masked as a way of making these compounds more stable.
COMPOUNDS, COMPOSITIONS, AND METHODS OF MAKING AND USING THE SAME
Compounds are provided according to Formula (I), and hydrates thereof, and compositions thereof; and methods of using and making the same. Compounds of the present invention are contemplated useful for suppressing pain during cosmetic, medical, and dental procedures. In another aspect, provided herein is a composition comprising the compound of Formula (I) or hydrate thereof and a pharmaceutically acceptable carrier.
COMPOUNDS, COMPOSITIONS, AND METHODS OF MAKING AND USING THE SAME
Compounds are provided according to Formula (I), and hydrates thereof, and compositions thereof; and methods of using and making the same. Compounds of the present invention are contemplated useful for suppressing pain during cosmetic, medical, and dental procedures. In another aspect, provided herein is a composition comprising the compound of Formula (I) or hydrate thereof and a pharmaceutically acceptable carrier.
Process for the preparation of Metaraminol
Object of the invention is a process for the preparation of Metaraminol and the salts thereof, in particular its pharmaceutically acceptable salts, especially Metaraminol bi-L-tartrate. Object of the invention is also the use of a novel catalyst and a novel ligand for the synthesis of Metaraminol and its salts.
Process for the preparation of Metaraminol
Object of the invention is a process for the preparation of Metaraminol and the salts thereof, in particular its pharmaceutically acceptable salts, especially Metaraminol bi-L-tartrate. Object of the invention is also the use of a novel catalyst and a novel ligand for the synthesis of Metaraminol and its salts.
Process for preparation of dexmethylphenidate hydrochloride
The present invention relates to a process for preparation of dexmethylphenidate hydrochloride from racemic methylphenidate. The process involves the treatment of racemic mixture of dl-threo-methylphenidate base in the presence of di-pivaloyl-D-tartaric acid (D-DPTA) in a solvent to isolate dipivaloyl tartrate salt of d-threo-methylphenidate. The dipivaloyl tartrate salt of d-threo-methylphenidate is treated with a base to obtain a d-threo-methylphenidate base, which is extracted using a suitable solvent. The d-threo-methylphenidate base is treated with hydrochloric acid-isopropyl alcohol solution to obtain slurry of d-threo-methylphenidate hydrochloride also known as dexmethylphenidate hydrochloride. The dexmethylphenidate hydrochloride slurry is filtered and washed with acetone. The invention also discloses a process for recovery of D-DPTA from the salt mother liquor and from the spent aqueous layer. The process is economical, environmental friendly and results in increased yield and optically pure dexmethylphenidate hydrochloride.
Process for preparation of dexmethylphenidate hydrochloride
The present invention relates to a process for preparation of dexmethylphenidate hydrochloride from racemic methylphenidate. The process involves the treatment of racemic mixture of dl-threo-methylphenidate base in the presence of di-pivaloyl-D-tartaric acid (D-DPTA) in a solvent to isolate dipivaloyl tartrate salt of d-threo-methylphenidate. The dipivaloyl tartrate salt of d-threo-methylphenidate is treated with a base to obtain a d-threo-methylphenidate base, which is extracted using a suitable solvent. The d-threo-methylphenidate base is treated with hydrochloric acid-isopropyl alcohol solution to obtain slurry of d-threo-methylphenidate hydrochloride also known as dexmethylphenidate hydrochloride. The dexmethylphenidate hydrochloride slurry is filtered and washed with acetone. The invention also discloses a process for recovery of D-DPTA from the salt mother liquor and from the spent aqueous layer. The process is economical, environmental friendly and results in increased yield and optically pure dexmethylphenidate hydrochloride.
LEVALBUTEROL SALT
Levalbuterol L-tartrate affords crystals possessing properties desirable for use in a metered dose inhaler.
LEVALBUTEROL SALT
Levalbuterol L-tartrate affords crystals possessing properties desirable for use in a metered dose inhaler.
Ligands for imaging cardiac innervation
Novel compounds that find use as imaging agents within nuclear medicine applications (PET imaging) for imaging of cardiac innervation are disclosed. These PET based radiotracers may exhibit increased stability, decreased NE release (thereby reducing side effects), improved quantitative data, and/or high affinity for VMAT over prior radiotracers. Methods of using the compounds to image cardiac innervation are also provided. In some instances the compounds are developed by derivatizing certain compounds with 18F in a variety of positions: aryl, alkyl, a keto, benzylic, beta-alkylethers, gamma-propylalkylethers and beta-proplylalkylethers. Alternatively or additionally, a methyl group a is added to the amine, and/or the catechol functionality is either eliminated or masked as a way of making these compounds more stable.