A61P5/38

Sulfur(VI) fluoride compounds and methods for the preparation thereof

This application describes a compound represented by Formula (I):
Yprivate use character BrketopenstZprivate use character ParenopenstX.sup.1S(O)(X.sup.2)F).sub.m].sub.n(I)
wherein: Y is a biologically active organic core group comprising one or more of an aryl group, a heteroaryl aryl group, a nonaromatic hydrocarbyl group, and a nonaromatic heterocyclic group, to which Z is covalently bonded; n is 1, 2, 3, 4 or 5; m is 1 or 2; Z is O, NR, or N; X.sup.1 is a covalent bond or CH.sub.2CH.sub.2, X.sup.2 is O or NR; and R comprises H or a substituted or unsubstituted group selected from an aryl group, a heteroaryl aryl group, a nonaromatic hydrocarbyl group, and a nonaromatic heterocyclic group. Methods of preparing the compounds, methods of using the compounds, and pharmaceutical compositions comprising the compounds are described as well.

ACTIVATOR OF PEROXISOME PROLIFERATOR-ACTIVATED RECEPTOR
20200268719 · 2020-08-27 ·

There is provided an activator of peroxisome proliferator-activated receptor which contains: a compound represented by the following Formula (I); a tautomer or stereoisomer of the compound; or a pharmaceutically acceptable salt or solvate thereof (where, in a case where R.sup.1, R.sup.2, R.sup.3, and R.sup.8 do not constitute a ring, in the Formula, R.sup.1, R.sup.2, R.sup.3, R.sup.6, R.sup.7, and R.sup.8 may be the same as or different from each other and represent a hydrogen atom, a halogen atom, an alkyl group having 1 to 8 carbon atoms, an alkoxy group having 1 to 8 carbon atoms, an alkyl group having 1 to 8 carbon atoms substituted with 1 to 3 halogen atoms, an alkoxy group having 1 to 8 carbon atoms substituted with 1 to 3 halogen atoms, a hydroxy group, an amino group, a carboxyl group, a mercapto group, an alkylsulfanyl group having 1 to 8 carbon atoms, a nitro group, or a cyano group).

Crystalline forms of a bromodomain and extraterminal protein inhibitor drug, processes for preparation thereof, and use thereof

The present disclosure relates to novel crystalline forms of a bromodomain protein inhibitor 2-[4-(2-hydroxyethoxy)-3,5-dimethylphenyl]-5,7-dimethoxyquinazolin-4(3H)-one and processes for preparation and use thereof, relating to pharmaceutical industry. Form CS2, Form CS8, Form CS13, Form CS20, Form CS1, Form CS7, Form CS9, Form CS11 and Form CS4 of the present disclosure can be used for preparing drugs treating cardiovascular, cholesterol or lipid-related disorders. ##STR00001##

Methods of using ZSCAN4 for rejuvenating human cells
10744183 · 2020-08-18 · ·

The present disclosure relates to methods for increasing telomere length in one or more human adult cells and/or increasing genome stability of one or more human adult cells, for example by contacting one or more human adult cells with an agent that increases expression of Zscan4 in the one or more human adult cells. Methods of treating a subject in need of telomere lengthening, treating a disease or condition associated with a telomere abnormality, of rejuvenating one or more human adult cells, of rejuvenating tissues or organs, and of rejuvenating a subject in need thereof, for example by contacting one or more human adult cells in the subject with an agent that increases expression of Zscan4, or by administering to a subject in need thereof, an agent that increases expression of Zscan4 is also provided.

SOLID DRUG FORM OF N-(2,6-BIS(1-METHYLETHYL)PHENYL)-N'-((1-(4-(DIMETHYLAMINO)PHENYL)CYCLOPENTYL)METHYL)UREA HYDROCHLORIDE AND COMPOSITIONS, METHODS AND KITS RELATED THERETO

A novel solid drug form of N-(2,6-bis(1-methylethyl)phenyl)-N-((1-(4-(dimethylamino)phenyl)cyclopentyl)methyl)urea hydrochloride (also referred to ATR-101) suitable for oral dosing, and to compositions, methods and kits relating thereto. ATR-101 has particular utility in the treatment of, for example, aberrant adrenocortical cellular activity, including adrenocortical carcinoma (ACC), congenital adrenal hyperplasia (CAH) and Cushing's syndrome.

SEMIFLUORINATED ALKANE COMPOSITIONS

The invention provides novel compositions comprising semifluorinated alkanes and at least one compound sensitive or prone to oxidation. The compositions can be used as medicines that are topically administered to an eye or ophthalmic tissue. The invention further provides kits comprising such compositions.

PD-1-BINDING MOLECULES AND METHODS OF USE THEREOF

The present invention is directed to selected anti-PD-1 antibodies capable of binding to both cynomolgus monkey PD-1 and to human PD-1: PD-1 mAb 1, PD-1 mAb 2, PD-1 mAb 3, PD-1 mAb 4, PD-1 mAb 5, PD-1 mAb 6, PD-1 mAb 7, PD-1 mAb 8, PD-1 mAb 9, PD-1 mAb 10, PD-1 mAb 11, PD-1 mAb 12, PD-1 mAb 13, PD-1 mAb 14, or PD-1 mAb 15, and to humanized and chimeric versions of such antibodies. The invention additionally pertains to PD-1-binding molecules that comprise PD-1 binding fragments of such anti-PD-1 antibodies, immunocongugates, and to bispecific molecules, including diabodies, BiTEs, bispecific antibodies, etc., that comprise (i) such PD-1-binding fragments, and (ii) a domain capable of binding an epitope of a molecule involved in regulating an immune check point present on the surface of an immune cells. The present invention also pertains to methods of using molecules that bind PD-1 for stimulating immune responses, as well as methods of detecting PD-1.

HUMAN ANTIBODIES AND BINDING FRAGMENTS THEREOF TO TENASCIN
20200223910 · 2020-07-16 ·

The present disclosure relates to antibodies and binding fragments to a Tenascin, in particular the FBG domain of a Tenascin, which are potentially less immunogenic than the parent antibody. The disclosure also relates to compositions comprising the antibody or binding fragment and use of any one of the same for diagnosis, prognosis and/or treatment of disorders such as those associated with chronic inflammation. The disclosure further provides methods of making the antibodies.

USES OF DPP IV INHIBITORS
20200222411 · 2020-07-16 ·

The specification describes the use of selected DPP IV inhibitors for the treatment of physiological functional disorders and for reducing the risk of the occurrence of such functional disorders in at-risk patient groups. In addition, the use of the above-mentioned DPP IV inhibitors in conjunction with other active substances is described, by means of which improved treatment outcomes can be achieved. These applications may be used to prepare corresponding medicaments.

Covalent inhibitors of PAD4

The present invention provides compounds of formula I useful as inhibitors of PAD4, compositions thereof, and methods of treating PAD4-related disorders. ##STR00001##