Patent classifications
C07D239/553
CANNABINOID COMPOSITIONS AND USE THEREOF
Methods of rapidly inhibiting efflux from a cell, sensitizing a drug-resistant cell to a drug and treating a subject with a drug-resistant pathology, by administering tetrahydrocannabinolic acid (THCa), cannabidiol (CBD) or a combination thereof are provided. Pharmaceutical compositions comprising THCa, CBD or a combination thereof and a drug are also provided.
PYRIMIDINEDIONE COMPOUNDS
Provided are novel pyrimidine dione compounds and pharmaceutically acceptable salts thereof, that are useful for the treatment of hypertrophic cardiomyopathy (HCM) and conditions associated with left ventricular hypertrophy or diastolic dysfunction. The synthesis and characterization of the compounds and pharmaceutically acceptable salts thereof, are described, as well as methods for treating HCM and other forms of heart disease.
PYRIMIDINEDIONE COMPOUNDS
Provided are novel pyrimidine dione compounds and pharmaceutically acceptable salts thereof, that are useful for the treatment of hypertrophic cardiomyopathy (HCM) and conditions associated with left ventricular hypertrophy or diastolic dysfunction. The synthesis and characterization of the compounds and pharmaceutically acceptable salts thereof, are described, as well as methods for treating HCM and other forms of heart disease.
METHOD FOR PRODUCING OROTIC ACID DERIVATIVE
Provided is a method for producing an orotic acid derivative, the method comprising a condensation step of performing, under a basic condition, a condensation reaction between an orotic acid halide represented by General Formula (I) and a compound represented by General Formula (II) to generate an orotic acid derivative represented by General Formula (III); and a neutralization crystallization step of precipitating crystals of orotic acid by neutralization crystallization to separate a liquid containing the orotic acid derivative from the crystals of orotic acid, after the condensation step. In General Formula (I), (II), or (III), X is a halogen atom, and A is a group represented by General Formula (A-1) or (A-2). In General Formula (A-1) or (A-2), R.sup.1 is a hydrogen atom or an organic group, and R.sup.2 and R.sup.3 are each independently an organic group. In a case where R.sup.1 is an organic group, R.sup.1 and R.sup.2 may be bonded to each other to form a ring.
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Process for the preparation of Tipiracil hydrochloride and intermediates thereof
The present invention provides a process for the preparation of Tipiracil HCl of Formula (I) and intermediate thereof with improved yields and purities. ##STR00001##
Process for the preparation of Tipiracil hydrochloride and intermediates thereof
The present invention provides a process for the preparation of Tipiracil HCl of Formula (I) and intermediate thereof with improved yields and purities. ##STR00001##
Processes for the preparation of uracil derivatives
The present invention relates to processes and intermediates for preparing Gonadotropin-Releasing Hormone (GnRH) receptor antagonists of structure (VI); and stereoisomers and pharmaceutically acceptable salts thereof.
Processes for the preparation of uracil derivatives
The present invention relates to processes and intermediates for preparing Gonadotropin-Releasing Hormone (GnRH) receptor antagonists of structure (VI); and stereoisomers and pharmaceutically acceptable salts thereof.
NUCLEOSIDE DERIVATIVE FOR PREVENTING AND TREATING INFLAMMATION AND APPLICATION THEREOF
The present invention provides a nucleoside derivative for preventing and treating inflammation and an application thereof in the preparation of a drug for preventing and treating inflammatory diseases. The nucleoside derivative for preventing and treating inflammation provided by the present invention can significantly ameliorate conditions of pancreatitis, hepatitis, arthritis and the like, ameliorate organ injury and inflammatory indexes, and have better effects than positive control drug, indometacin. Compared with the conventional anti-inflammatory drugs, aspirin, ibuprofen, indomethacin, phenylbutazone, diclofenac, piroxicam and glucocorticoids, the nucleoside derivative for preventing and treating inflammation provided by the present invention has the advantage of significantly fewer side effects.
PROCESS FOR THE SYNTHESIS OF THE SODIUM SALT OF 4-[[(1R)-2-[5-(2-FLUORO-3-METHOXYPHENYL)-3-[[2-FLUORO-6-(TRIFLUOROMETHYL)-PHENYL]METHYL]-3,6-DIHYDRO-4-METHYL-2,6- DIOXO-1(2H)-PYRIMIDINYL]-1- PHENYLETHYL]AMINO]-BUTANOIC ACID (ELAGOLIX SODIUM SALT) AND INTERMEDIATES OF SAID PROCESS
The present invention to a process for the preparation of the sodium salt of 4-[[(1R)-2-[5-(2-fluoro-3-methoxyphenyl)-3-[[2-fluoro-6-(trifluoromethyl)phenyl]methyl]-3,6-dihydro-4-methyl-2,6-dioxo-1(2H)-pyrimidinyl]-1-phenylethyl]-amino]-butanoic acid, compound also known as Elagolix sodium salt, having the formula (I) reported below:
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