C07J41/0005

SQUALAMINE SOLID FORMS AND METHODS OF MAKING THE SAME
20210332079 · 2021-10-28 · ·

Provided herein are crystalline solid forms of squalamine phosphate designated as Form 1 and Form 2, compositions containing one or both forms, and methods of their preparation and of their use.

NEUROACTIVE 19-ALKOXY-17-SUBSTITUTED STEROIDS, PRODRUGS THEREOF, AND METHODS OF TREATMENT USING SAME
20210308149 · 2021-10-07 ·

The present disclosure is generally directed to neuroactive 19-alkoxy-17-substituted steroids as referenced herein, and pharmaceutically acceptable salts thereof, for use as, for example, an anesthetic, and/or in the treatment of disorders relating to GABA function and activity. The present disclosure is further directed to pharmaceutical compositions comprising such compounds.

Crystalline forms of a fatty acid bile acid conjugate, preparation method thereof and use thereof

The present disclosure relates to novel crystalline forms of compound (I) and processes for preparation and use thereof. Crystalline forms CS3, CS2, CS5 and CS8 of compound (I) of the present disclosure have advantages in at least one aspect of solubility, stability, melting point, hygroscopicity, particle size, bioavailability, processability, purification effect, flowability, adhesiveness, stability in drug product, in vitro and in vivo dissolution, etc., which provides new and better choices for preparation of drug product containing compound (I) and has significant values for future drug development. ##STR00001##

Crystalline forms of a fatty acid bile acid conjugate, preparation method thereof and use thereof

The present disclosure relates to novel crystalline forms of compound (I) and processes for preparation and use thereof. Crystalline forms CS3, CS2, CS5 and CS8 of compound (I) of the present disclosure have advantages in at least one aspect of solubility, stability, melting point, hygroscopicity, particle size, bioavailability, processability, purification effect, flowability, adhesiveness, stability in drug product, in vitro and in vivo dissolution, etc., which provides new and better choices for preparation of drug product containing compound (I) and has significant values for future drug development. ##STR00001##

Polyethylene Glycol-Conjugated Glucocorticoid Prodrugs and Compositions and Methods Thereof
20210252018 · 2021-08-19 ·

Polyethylene glycol (PEG)-conjugated glucocorticoid prodrugs, methods of preparation, and use for the treatment of diseases and disorders are disclosed. In particular, PEG-conjugated dexamethasone compounds and methods of using them for treating inflammatory and autoimmune diseases, including but not limited to lupus, are disclosed.

Squalamine solid forms and methods of making the same
11066438 · 2021-07-20 · ·

Provided herein are crystalline solid forms of squalamine phosphate designated as Form 1 and Form 2, compositions containing one or both forms, and methods of their preparation and of their use.

COMPOUNDS, COMPOSITIONS, AND METHODS FOR TREATMENT OF ANDROGEN-MEDIATED DISEASE

Provided herein are steroid sulfatase inhibitor compounds and androgen receptor inhibitor compounds that can be useful in, for example, the treatment of cancers such as prostate cancer and breast cancer. Pharmaceutical compositions and kits including the compounds are described, as well as methods for the treatment of cancer such as prostate cancer and breast cancer.

ARAMCHOL SALTS

The present invention relates to salts of arachidyl amido cholanoic acid (Aramchol), pharmaceutical compositions comprising Aramchol salts, methods for their preparation, and methods of use thereof in medical treatment.

NEUROACTIVE STEROIDS, COMPOSITIONS, AND USES THEREOF

Compounds are provided according to Formula (I):

##STR00001##

and pharmaceutically acceptable salts thereof, wherein Z is a group of the formula (i), (ii), (iii), (iv), or (v):

##STR00002##

and wherein L.sup.1, L.sup.2, L.sup.3, X.sup.1, X.sup.2, Y, R.sup.Z4, R.sup.Z5, R.sup.Z6, n, R.sup.1, R.sup.2, R.sup.3a, R.sup.3b, R.sup.4a, R.sup.4b, R.sup.6a, R.sup.6b, R.sup.7a, R.sup.7b, R.sup.11a, R.sup.11b, R.sup.14, R.sup.17, R.sup.19, R.sup.20, R.sup.23a, R.sup.23b, and R.sup.24 are as defined herein, and pharmaceutical compositions thereof. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of CNS-related conditions in mammals.

CRYSTALLINE FORMS OF A FATTY ACID BILE ACID CONJUGATE, PREPARATION METHOD THEREOF AND USE THEREOF
20210147471 · 2021-05-20 ·

The present disclosure relates to novel crystalline forms of compound (I) and processes for preparation and use thereof. Crystalline forms CS3, CS2, CS5 and CS8 of compound (I) of the present disclosure have advantages in at least one aspect of solubility, stability, melting point, hygroscopicity, particle size, bioavailability, processability, purification effect, flowability, adhesiveness, stability in drug product, in vitro and in vivo dissolution, etc., which provides new and better choices for preparation of drug product containing compound (I) and has significant values for future drug development.

##STR00001##