C07F9/3834

COMPOSITIONS AND METHODS FOR USING FIXED BIOLOGICAL SAMPLES IN PARTITION-BASED ASSAYS

The present disclosure provides compositions and methods for using fixed biological samples in partition-based assays. In at least one embodiment, the disclosure provides a composition comprising a fixed biological sample and an un-fixing agent contained in a partition, such as a discrete droplet. In some embodiments, the disclosure provides un-fixing agent compounds capable of catalytically cleaving crosslinks in fixed biological samples, particularly crosslinked nucleic acids, such as RNA.

BICYCLIC ARYL SPHINGOSINE 1-PHOSPHATE ANALOGS

Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at S1P receptors.

Compounds and methods for inhibiting NHE-mediated antiport in the treatment of disorders associated with fluid retention or salt overload and gastrointestinal tract disorders

The present disclosure is directed to compounds and methods for the treatment of disorders associated with fluid retention or salt overload, such as heart failure (in particular, congestive heart failure), chronic kidney disease, end-stage renal disease, liver disease, and peroxisome proliferator-activated receptor (PPAR) gamma agonist-induced fluid retention. The present disclosure is also directed to compounds and methods for the treatment of hypertension. The present disclosure is also directed to compounds and methods for the treatment of gastrointestinal tract disorders, including the treatment or reduction of pain associated with gastrointestinal tract disorders. The methods generally comprise administering to a mammal in need thereof a pharmaceutically effective amount of a compound, or a pharmaceutical composition comprising such a compound, that is designed to be substantially active in the gastrointestinal (GI) tract to inhibit NHE-mediated antiport of sodium ions and hydrogen ions therein. More particularly, the method comprises administering to a mammal in need thereof a pharmaceutically effective amount of a compound, or a pharmaceutical composition comprising such a compound, that inhibits NHE-3, -2 and/or -8 mediated antiport of sodium and/or hydrogen ions in the GI tract and is designed to be substantially impermeable to the layer of epithelial cells, or more specifically the epithelium of the GI tract. As a result of the compound being substantially impermeable, it is not absorbed and is thus essentially systemically non-bioavailable, so as to limit the exposure of other internal organs (e.g., liver, heart, brain, etc.) thereto. The present disclosure is still further directed to a method wherein a mammal is administered such a compound with a fluid-absorbing polymer, such that the combination acts as described above and further provides the ability to sequester fluid and/or salt present in the GI tract.

SYNERGISTIC CANNABINOID ESTERS, THEIR SALTS AND USES THEREOF
20240189327 · 2024-06-13 ·

Cannabinoid esters and their soluble salts with synergistic or additive therapeutic counterparts and stable formulations thereof, as well as their edible, beverage and medicinal applications. The synergistic or additive cannabinoid esters may be used as drugs or prodrugs for treating various conditions related to the modulation or biased modulation of cannabinoid receptors, including but not limited to, pain and inflammation, arthritis, cancer, glaucoma, neurodegenerative disorders, multiple sclerosis, renal fibrosis, fibrotic disorder, mental health disorders, addiction, motor function disorders and gastrointestinal and metabolic disorders.

Quinazoline and Indole Compounds to Treat Medical Disorders

Compounds, methods of use, and processes for making inhibitors of Complement Factor B are provided.

Activators of glucokinase

The present invention provides for novel compounds of Formulas I and II and pharmaceutically acceptable salts and co-crystals thereof which have glucokinsae activator activity. The present invention further provides for pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucokinase activator is indicated, including Type 1 and 2 diabetes, impaired glucose tolerance, insulin resistance and hyperglycemia. The present invention also provides for processes of making the compounds of Formulas I and II, including salts and co-crystals thereof, and pharmaceutical compositions comprising the same.

CONJUGATE AND THE PREPARING METHOD AND USE THEREOF
20240261425 · 2024-08-08 · ·

A conjugate may have formula (1), i.e., M-[(L1).sub.a-(L2).sub.b-(D).sub.c] (1), wherein M is a biological macromolecule having a nucleophilic functional group, M is linked to L1 with the nucleophilic functional of M, D is a functional molecule, L2 is a linker, and L1 is a compound of formula 1

##STR00001##

wherein R is F or OH, and L2 is linked to R.sub.1, R.sub.3 or R.sub.2, a is an integer of 1 to 10, b, c is each independently an integer of 0 to 10, provided that b and c are not simultaneously 0. R.sub.1, R.sub.2, and R.sub.3, may independently be H, optionally substituted alkyl, or optionally substituted aryl, and R.sub.1, may be H or isotope thereof ? C may link R.sub.1 and a C linking R.sub.2 form a ring.

Modified graphene, method of producing modified graphene, modified graphene-resin composite, modified graphene sheet, and modified graphene dispersion

The modified graphene includes a structure represented by the following formula (I), wherein the modified graphene has a ratio (g/d) of an intensity g of a G band to an intensity d of a D band of 1.0 or more in a Raman spectroscopy spectrum thereof:
Gr1-Ar1-X1-(Y1).sub.n1(I)
in the formula (I), Gr1 represents a single-layer graphene or a multilayer graphene, Ar1 represents an arylene group having 6 to 18 carbon atoms, X1 represents a single bond, a linear, branched, or cyclic alkylene group having 1 to 20 carbon atoms, or a group obtained by substituting at least one carbon atom in a linear, branched, or cyclic alkylene group having 1 to 20 carbon atoms with at least one structure selected from the group consisting of O, NH, ##STR00001##
CO, COO, CONH, and an arylene group.

INFRARED-ABSORBING COMPOSITION, INFRARED-CUT FILTER, AND IMAGING OPTICAL SYSTEM
20180275326 · 2018-09-27 ·

An infrared-absorbing composition according to the present invention includes: an infrared absorber formed by a phosphonic acid represented by the following formula (a) and copper ion; and a phosphoric acid ester allowing the infrared absorber to be dispersed. The phosphoric acid ester includes at least one of a phosphoric acid diester and a phosphoric acid monoester. R.sub.1 is a phenyl group or a phenyl group in which at least one hydrogen atom is substituted by a halogen atom. When molar contents of the phosphonic acid, the copper ion, and the phosphoric acid ester are respectively defined as C.sub.A mol, C.sub.C mol, and C.sub.E mol and a total molar content of reactive hydroxy groups is defined as C.sub.H mol, the relations C.sub.A/C.sub.E<1 and C.sub.H/C.sub.C>1.95 are satisfied.

##STR00001##

Flame-retardant expandable polymers

The present relates to flame-retardant expandable polymers and to polymer foams and to the use thereof. These flame-retardant expandable polymers and polymer foams can be contained in one or several pressurized containers. According to the present, at least one of the following phosphorus compounds is used as a flame retardant: phosphorus compound according to formula (Ia): (Ia) 10-hydroxy-9, 10-dihydro-9-oxa-10-phosphaphenanthrene-10-oxide (DOPO-OH); or the salts thereof according to formula (Ib): (Ib) (DOPO-OR); or the ring-opened hydrolysates thereof according to formula (Ic): (Ic).