Patent classifications
C07C59/255
SELECTIVE SEROTONIN 2A/2C RECEPTOR INVERSE AGONISTS AS THERAPEUTICS FOR NEURODEGENERATIVE DISEASES
Behavioral pharmacological data with the compound of formula (1), a novel and selective 5HT2A/2C receptor inverse agonist, demonstrate in vivo efficacy in models of psychosis and dyskinesias. This includes activity in reversing MK-801 induced locomotor behaviors, suggesting that this compound may be an efficacious anti-psychotic, and activity in an MPTP primate model of dyskinesias, suggesting efficacy as an anti-dyskinesia agent. These data support the hypothesis that SHT2A/2C receptor inverse agonism may confer antipsychotic and anti-dyskinetic efficacy in humans, and indicate a use of the compound of formula (I) and related agents as novel therapeutics for Parkinson's Disease, related human neurodegenerative diseases, and psychosis.
Ferric Organic Compounds, Uses Thereof and Methods of Making Same
The present invention discloses a novel form of ferric organic compounds, including a form of ferric citrate, which are soluble over a wider range of pH, and which have a large active surface area. The ferric organic compounds of the present invention can be delivered effectively by oral route with better delivery to treat patients suffering from hyperphosphatemia, metabolic acidosis and other disorders responsive to ferric organic compound therapy.
Ferric Organic Compounds, Uses Thereof and Methods of Making Same
The present invention discloses a novel form of ferric organic compounds, including a form of ferric citrate, which are soluble over a wider range of pH, and which have a large active surface area. The ferric organic compounds of the present invention can be delivered effectively by oral route with better delivery to treat patients suffering from hyperphosphatemia, metabolic acidosis and other disorders responsive to ferric organic compound therapy.
Solid forms of stemospironine and its salts
Disclosed are stemospironine salts of Formula 1: wherein HX represents HCl, HBr, L-tartaric acid, D-tartaric acid, sulfuric acid, (+)-(1S)-10-camphorsulfonic acid, ethanesulfonic acid and ethane-1,2-disulfonic acid. This invention also provides crystalline polymorph forms of the compound of Formula 1 wherein HX is HCl, stemospironine hydrochloride. This invention also provides a new crystalline form of the compound of Formula 2, stemospironine free base: Also disclosed are compositions containing one or more compounds of Formula 1, methods for controlling cough comprising administering a therapeutically effective amount of a compound of Formula 1, and methods for preparing compounds of Formula 1. Also disclosed is a method for preparing crystalline stemospironine hydrochloride polymorph Form II from stemospironine hydrochloride polymorph Form I. ##STR00001##
Solid forms of stemospironine and its salts
Disclosed are stemospironine salts of Formula 1: wherein HX represents HCl, HBr, L-tartaric acid, D-tartaric acid, sulfuric acid, (+)-(1S)-10-camphorsulfonic acid, ethanesulfonic acid and ethane-1,2-disulfonic acid. This invention also provides crystalline polymorph forms of the compound of Formula 1 wherein HX is HCl, stemospironine hydrochloride. This invention also provides a new crystalline form of the compound of Formula 2, stemospironine free base: Also disclosed are compositions containing one or more compounds of Formula 1, methods for controlling cough comprising administering a therapeutically effective amount of a compound of Formula 1, and methods for preparing compounds of Formula 1. Also disclosed is a method for preparing crystalline stemospironine hydrochloride polymorph Form II from stemospironine hydrochloride polymorph Form I. ##STR00001##
Solid forms of stemospironine and its salts
Disclosed are stemospironine salts of Formula 1: wherein HX represents HCl, HBr, L-tartaric acid, D-tartaric acid, sulfuric acid, (+)-(1S)-10-camphorsulfonic acid, ethanesulfonic acid and ethane-1,2-disulfonic acid. This invention also provides crystalline polymorph forms of the compound of Formula 1 wherein HX is HCl, stemospironine hydrochloride. This invention also provides a new crystalline form of the compound of Formula 2, stemospironine free base: Also disclosed are compositions containing one or more compounds of Formula 1, methods for controlling cough comprising administering a therapeutically effective amount of a compound of Formula 1, and methods for preparing compounds of Formula 1. Also disclosed is a method for preparing crystalline stemospironine hydrochloride polymorph Form II from stemospironine hydrochloride polymorph Form I. ##STR00001##
AXL kinase inhibitors and use of the same
Tartrate salts of the compound of structure (I), ##STR00001##
crystalline forms thereof, and therapeutic applications thereof for treating solid tumors (e.g., advanced solid tumor) or hematopoietic cancers. Also provided herein are methods for synthesizing the tartrate salts and the crystalline forms thereof.
VARENICLINE COMPOUND AND PROCESS OF MANUFACTURE THEREOF
The present disclosure relates to the field of synthesizing substantially pure varenicline and its intermediates. It also relates to the pharmaceutical compositions comprising varenicline and the method of use of these pharmaceutical compositions for smoking cessation.
SELECTIVE ANDROGEN RECEPTOR DEGRADER (SARD) LIGANDS AND METHODS OF USE THEREOF
This invention is directed to pyrrole, pyrazole, imidazole, triazole, and morpholine based selective androgen receptor degrader (SARD) compounds including cyclic and heterocyclic anilide rings and their synthetic precursors, and mono-, di-, or multi-substituted N-heterocyclic rings, R-isomers, non-hydroxylated and/or non-chiral propanamides in treating androgen receptor dependent diseases and conditions such as hyperproliferations of the prostate including pre-malignancies and benign prostatic hyperplasia, prostate cancer, advanced prostate cancer, castration resistant prostate cancer, triple negative breast cancer, other cancers expressing the androgen receptor, androgenic alopecia or other hyperandrogenic dermal diseases, Kennedy's disease, amyotrophic lateral sclerosis (ALS), abdominal aortic aneurysm (AAA), and uterine fibroids, and to methods for reducing the levels of androgen receptor-full length (AR-FL) including pathogenic or resistance mutations, AR-splice variants (AR-SV), and pathogenic polyglutamine (polyQ) polymorphisms of AR in a subject.
SELECTIVE ANDROGEN RECEPTOR DEGRADER (SARD) LIGANDS AND METHODS OF USE THEREOF
This invention is directed to pyrrole, pyrazole, imidazole, triazole, and morpholine based selective androgen receptor degrader (SARD) compounds including cyclic and heterocyclic anilide rings and their synthetic precursors, and mono-, di-, or multi-substituted N-heterocyclic rings, R-isomers, non-hydroxylated and/or non-chiral propanamides in treating androgen receptor dependent diseases and conditions such as hyperproliferations of the prostate including pre-malignancies and benign prostatic hyperplasia, prostate cancer, advanced prostate cancer, castration resistant prostate cancer, triple negative breast cancer, other cancers expressing the androgen receptor, androgenic alopecia or other hyperandrogenic dermal diseases, Kennedy's disease, amyotrophic lateral sclerosis (ALS), abdominal aortic aneurysm (AAA), and uterine fibroids, and to methods for reducing the levels of androgen receptor-full length (AR-FL) including pathogenic or resistance mutations, AR-splice variants (AR-SV), and pathogenic polyglutamine (polyQ) polymorphisms of AR in a subject.