C07D207/28

PANTETHEINE DERIVATIVES AND USES THEREOF

The present disclosure relates to compounds of Formula (I), (II), or (II′): (I), (II), (II′), and pharmaceutically acceptable salts or solvates thereof. The present disclosure also relates to pharmaceutical compositions comprising the compounds and therapeutic and diagnostic uses of the compounds and pharmaceutical compositions.

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METHODS OF PREPARING CHIRAL BENZODIAZEPINONE DERIVATIVES

The present invention provides methods of preparing compound of Formula (I), wherein the compounds are represented by the structure of Formula (I) wherein: R.sup.1 each is independently F, Cl, Br, I, OCH.sub.3, CN or NO.sub.2; R.sup.2 each is independently identical or different C.sub.1-C.sub.5 alkyl; n.sup.1 is an integer between 1 and 5; and n.sup.2 is an integer between 1 and 4. In addition, the present invention provides a compound represented by the following structures: Compound (1a) and Compound (2), wherein X comprises: chloride, acetate, adipate, alginate, ascorbate, aspartate, benzoate, benzenesulfonate, bisulfate, borate, butyrate, citrate, camphorate, camphorsulfonate, cyclopentanepropionate, digluconate, dodecylsulfate, ethanesulfonate, fumarate, glucoheptanoate, glycerophosphate, hemisulfate, heptanoate, hexanoate, hydroiodide, maleate, 2-hydroxyethanesulfonate, lactate, methanesulfonate, 2-naphthalenesulfonate, nicotinate, nitrate, oxalate, pectinate, persulfate, 3-phenylpropionate, phosphate, picrate, pivalate, propionate, salicylate, succinate, sulfate, sulfonate, tartrate, thiocyanate, toluene sulfonate, or undecanoate salt, or any combination thereof.

SOLID FORMS OF FASORACETAM

The disclosure is directed to cocrystals of fasoracetam, including R-fasoracetam, and various coformers. Crystalline materials comprising fasoracetam, including R-fasoracetam, are also provided. The disclosure further includes pharmaceutical compositions and methods of treatment of the cocrystals and crystalline materials of the disclosure.

Substituted Heterocyclic Derivative, Preparation Method And Use Thereof
20170334896 · 2017-11-23 ·

The invention provides a compound as shown by Formula I having an enzyme activity which can inhibit endocannabinoid hydrolases NAAA and/or FAAH, or a pharmaceutically acceptable salt, hydrate or solvate thereof, and a preparation method and a use of the compound.

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Substituted Heterocyclic Derivative, Preparation Method And Use Thereof
20170334896 · 2017-11-23 ·

The invention provides a compound as shown by Formula I having an enzyme activity which can inhibit endocannabinoid hydrolases NAAA and/or FAAH, or a pharmaceutically acceptable salt, hydrate or solvate thereof, and a preparation method and a use of the compound.

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Process and intermediates for the synthesis of 8-[{1-(3,5-bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one compounds

This application discloses a novel process to synthesize 8-[{1-(3,5-Bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one compounds, which may be used, for example, as NK-1 inhibitor compounds in pharmaceutical preparations, intermediates useful in said process, and processes for preparing said intermediates; also disclosed is a process for removal of metals from N-heterocyclic carbine metal complexes.

Process and intermediates for the synthesis of 8-[{1-(3,5-bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one compounds

This application discloses a novel process to synthesize 8-[{1-(3,5-Bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one compounds, which may be used, for example, as NK-1 inhibitor compounds in pharmaceutical preparations, intermediates useful in said process, and processes for preparing said intermediates; also disclosed is a process for removal of metals from N-heterocyclic carbine metal complexes.

PYRROLIDONE DERIVATIVES, OLIGOMERS AND POLYMERS

Simple organic structures, organic/inorganic polymers, and other substrates have been made, all of which have at least one pyrrolidone moiety present, and found to exhibit low toxicity, low complement activation features and may be used to reduce protein interactions with drug conjugates while enhancing in vivo residency times for these conjugates when used as an injectable composition; thus these compounds can be used as substitutes for PEG in PEGaylation. Surprisingly, these compounds also exhibit unique intrinsic fluorescence (IF) or non-traditional fluorescence (NTF) properties that currently cannot be explained by traditional photochemistry and fluorescence paradigms are described. These compounds have a variety of applications such as in cellular imaging, gene transfection, bio-diagnostics, biosensing, fluorescence directed surgical resections, drug delivery, forensics, environmental diagnostics, mineral/gemstone characterization, counterfeit goods detection, tracer studies related to liquid/water flow, oil field enhancements and diagnostics, prevention of photo-bleaching, and LED display enhancements and others.

CRYSTALLINE FORMS OF HYDROXYNORKETAMINE

The present invention provides novel, stable, processable and pharmaceutically acceptable salt forms of 2R,6R-hydrox-ynorketamineor 2S,6S-hydroxynorketamine with high aqueous solubility.

CRYSTALLINE FORMS OF PARP INHIBITORS

The present disclosure relates to crystalline forms of 4,5,6,7-tetrahydro-11-methoxy-2-[(4-methyl-1-piperazinyl)methyl]-1H-cyclopenta[a]pyrrolo[3,4-c]carbazole-1,3(2H)-dione, including salts forms and free base forms.