Patent classifications
C07B2200/13
Processes and intermediates for the preparation of soluble guanylate cyclase stimulators
The present disclosure relates to novel processes for the preparation of compounds of Formula I. Some of these compounds are useful as stimulators of soluble guanylate cyclase (sGC). Others are useful intermediates towards the preparation of said stimulators. These processes are amenable to large scale preparation and produce stable 3-(2-pyrimidinyl)pyrazoles of Formula I in high purity and yields. The present invention has the additional advantage of facile reaction conditions, amenable to scale up for large scale manufacturing. The disclosure also provides novel intermediates useful in the preparation of said compounds. ##STR00001##
Process for making beta 3 agonists and intermediates
The present invention is directed to processes for preparing beta 3 agonists of Formula (I) and Formula (II) and their intermediates. The beta 3 agonists are useful in the treatment of certain disorders, including overactive bladder, urinary incontinence, and urinary urgency.
METHOD FOR PREPARING AN ANTIFIBROTIC AGENT
The present invention relates to a process for the preparation of pirfenidone, an immunosuppressive drug developed for the treatment of idiopathic pulmonary fibrosis.
HETEROCYCLIC COMPOUNDS AS PI3K-y INHIBITORS
This application relates to compounds of Formula (I):
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or pharmaceutically acceptable salts or stereoisomers thereof, which are inhibitors of PI3K-γ which are useful for the treatment of disorders such as autoimmune diseases, cancer, cardiovascular diseases, and neurodegenerative diseases.
PROCESS FOR THE PREPARATION OF NOVEL POLYMORPHIC FORMS OF 5-FLUORO-1,3-DIHYDRO-1-HYDROXY-2,1- BENZOXABOROLE
Novel polymorphic forms of tavaborole, Form A and Form B, and methods of making same are disclosed. Methods are disclosed for the manufacture of the novel polymorphic Forms A and B. Methods include dissolving tavaborole in a pharmaceutically acceptable solvent to obtain a mixture, heating the mixture until a clear solution is obtained, cooling the clear solution, stirring the clear solution to obtain a crystalline product, filtering the crystalline product, and drying the crystalline product to obtain the pharmaceutically acceptable crystalline form of tavaborole. Pharmaceutical composition are disclosed including a pharmaceutically acceptable crystalline form of tavaborole Form A and/or Form B.
Polymorphic forms of RAD1901-2HCL
Various polymorphic forms of RAD1901-2HCl, including three crystalline and amorphous forms, are prepared and characterized. Uses of the various polymorphic forms of RAD1901-2HCl for cancer treatment are also disclosed.
COMPOSITIONS AND METHODS AND USES RELATING THERETO
Stable crystal forms comprising lithium ions and the conjugate base of an organic acid which is in the form of anhydrous coordination polymer that exhibit improved in vivo performance with respect to lithium carbonate.
Crystal Forms of Crisaborole In Free Form And Preparation Method And Use Thereof
The present invention relates to four crystal forms of crisaborole in free form and the preparation method thereof. The present invention also relates to the pharmaceutical composition containing the crystal forms and the use thereof.
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SYNTHETIC METHODS FOR PREPARATION OF 4-(2-CHLORO-4-METHOXY-5-METHYLPHENYL)-N-[(1S)-2-CYCLOPROPYL-1-(3-FLUORO-4-METHYLPHENYL)ETHYL]-5-METHYL-N-PROP-2-YNYL-1,3-THIAZOL-2-AMINE
The present disclosure relates to the fields of chemistry and medicine, more particularly to processes for making 4-(2-chloro-4-methoxy-5-methylphenyl)-N-[(1S)-2-cyclopropyl-1-(3-fluoro-4-methylphenyl)ethyl]-5-methyl-N-prop-2-ynyl-1,3-thi-azol-2-amine (Compound 1), pharmaceutically acceptable salts, and crystalline forms thereof, for the treatment of congenital adrenal hyperplasia (CAH).
FORMULATIONS COMPRISING HETEROCYCLIC PROTEIN KINASE INHIBITORS
Provided is a composition comprising a polyglycolized glyceride and a compound having the following structure (I):
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or a pharmaceutically acceptable salt thereof. Also provided are crystalline forms of the compound of structure (I), or a pharmaceutically acceptable salt thereof. Methods of making the same, and methods for using the same in the treatment of cancer, autoimmune, inflammatory and other Pim kinase-associated diseases, disorders or conditions are also disclosed.