C07J5/00

NON-HORMONAL STEROID MODULATORS OF NF-kB FOR TREATMENT OF DISEASE
20210052606 · 2021-02-25 ·

The present invention relates to compounds and methods which may be useful as treatments of neuromuscular diseases such as muscular dystrophy, and as inhibitors of NF-B for the treatment or prevention of muscular wasting disease, including muscular dystrophy.

Non-hormonal steroid modulators of NF-kB for treatment of disease

Provided herein is a pharmaceutical composition comprising a compound having the structural formula ##STR00001##
wherein the compound is present in an amount effective to treat or reduce the symptoms of muscular dystrophy. The therapeutically effective amount may be between 10 mg to 200 mg, or may be between 0.01 mg/kg to 10.0 mg/kg. Also provided are methods of treating or reducing the symptoms of muscular dystrophy, comprising the administration, to a patient in need thereof, of a therapeutically effective of the above compound.

METHODS FOR PREPARING BILE ACIDS
20200369712 · 2020-11-26 ·

The present disclosure provides methods of preparing cholic acid, deoxycholic acid, or chenodeoxycholic acid, an ester thereof, or a pharmaceutically or cosmetically acceptable salt thereof, and novel and useful synthetic intermediates, for example, as described for methods 1, 1A, 1B, 2, 3, 3A, and 4. The method can start with a plant derived steroid as a starting material, such as dehydroepiandrosterone (DHEA) or Acetyl-dehydroepiandrosterone (Ac-DHEA). Also provided are pharmaceutical or cosmetic compositions and uses thereof, which comprise one or more of cholic acid, deoxycholic acid, or chenodeoxycholic acid, an ester thereof, or a pharmaceutically or cosmetically acceptable salt thereof, which is of high purity, for example, free of animal derived impurities.

POLYSUBSTITUTED BENZENE, PREPARATION METHOD THEREOF, AND METHOD OF USING THE SAME
20200361893 · 2020-11-19 ·

A polysubstituted benzene compound, preparation method thereof, and method of using the same. The compound has a formula I or I, where X represents carbon, sulfur, or oxygen; R.sup.1 represents a C.sub.1-16 alkyl, C.sub.2-16 alkenyl, or C.sub.2-10 alkynyl; R.sup.2 represents hydrogen, halogen, C.sub.1-16 alkyl, C.sub.2-16 alkenyl, or C.sub.2-10 alkynyl; or an aryl group or a substituted aryl group by 1-5 groups selected from halogen, C.sub.1-26 alkyl, C.sub.1-3 halogenated alkyl, OC.sub.1-3 alkyl, hydroxyl, amino, nitro, cyano group, aldehyde group and ester group; or a heteroaryl group or a substituted heteroaryl group by 1-5 groups selected from halogen, C.sub.1-26 alkyl, C.sub.1-3 halogenated alkyl, OC.sub.1-3 alkyl, hydroxyl, amino, nitro, cyano group, aldehyde group and ester group; the heteroaryl group is a 3-10-membered heteroaryl group including N, S, O, or a combination thereof.

OPHTHALMIC AQUEOUS COMPOSITION

An ophthalmic aqueous composition comprises levofloxacin, a salt thereof, or a solvate thereof; dexamethasone, an ester thereof, or a salt thereof; and one or at least two isotonic agents. The ophthalmic aqueous composition is substantially free of sodium chloride. This ophthalmic aqueous composition is excellent in drug stability and drug migration and has a clear appearance.

Cocrystal of progesterone and preparation method and use thereof

The present invention relates to a cocrystal of progesterone, which is formed by the active ingredient progesterone and a cocrystal former which is selected from isophthalic acid, 4-formylbenzeneboronic acid and 3-nitrophthalic acid. The present invention also relates to the method for preparing the cocrystal of progesterone and use thereof for increasing the thickness of endometrium, improving progesterone's solubility or increasing progesterone's permeation rate.

Lipid-linked prodrugs

This invention provides lipid-linked prodrugs having structures as set out herein. Uses of such lipid-linked prodrug compounds for treatment of various indications, and methods for making and using lipid-linked prodrugs are also provided.

Ophthalmic aqueous composition

An ophthalmic aqueous composition comprises levofloxacin, a salt thereof, or a solvate thereof; dexamethasone, an ester thereof, or a salt thereof; and one or at least two isotonic agents. The ophthalmic aqueous composition is substantially free of sodium chloride. This ophthalmic aqueous composition is excellent in drug stability and drug migration and has a clear appearance.

Neuroactive steroids, compositions, and uses thereof

Described herein are steroids of Formula (I): ##STR00001##
and pharmaceutically acceptable salts thereof; wherein R.sup.1, R.sup.2a, R.sup.2b, R.sup.3, R.sup.4, R.sup.5a, R.sup.5b, R.sup.6, and Z are as defined herein. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, convulsive disorders, disorders of memory and/or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and/or withdrawal syndromes, and tinnitus.

Enzymatic process for obtaining 17 alpha-monoesters of cortexolone and/or its 9,11-dehydroderivatives
10716796 · 2020-07-21 · ·

The present invention refers to a new enzymatic process for obtaining 17-monoesters of cortexolone and/or its 9,11-dehydroderivatives starting from the corresponding 17,21-diesters which comprises an enzymatic alcoholysis reaction. Furthermore, the present invention refers to new crystalline forms of cortexolone-17-propionate and 9,11-dehydro-cortexolone 17-butanoate.