Patent classifications
C07C2601/18
Zwitterion-ruthenium complex for catalytic aerobic oxidation reactions
Zwitterion ligand metal complexes and methods of aerobic oxidation using a zwitterion ligand metal complex are provided. The zwitterion ligand metal complexes can include a transition metal salt and a zwitterion ligand, which can comprise a non-conjugated amide anion-phosphonium cation, an amide anion-ammonium cation, or an iminium cation. The methods of aerobic oxidation can include combining the zwitterion ligand metal complex with an oxidizable compound and molecular oxygen to allow the isolation of an oxidized compound from the oxidizable compound.
Monosubstituted or polysubstituted amphiphilic hypocrellin derivative, and preparation method and application thereof
The invention discloses a monosubstituted or polysubstituted amphiphilic hypocrellin derivative, and a preparation method and application thereof. The amphiphilic hypocrellin derivative substituted by a group containing PEG, a quaternary ammonium salt or the like prepared according to the invention has an obvious red shift in its absorption spectrum and a significantly enhanced molar extinction coefficient, compared with the parent hypocrellin, can efficiently produce singlet state oxygen and other reactive oxygen species under photosensitive conditions; has different amphiphilicities and increased biocompatibility with cells or tissues by regulating its hydrophilicity and hydrophobicity; can meet the requirements of different clinical drugs, and solves the requirements of different drug delivery methods for different drug hydrophilicity and lipophilicity. Under identical conditions, the amphiphilic hypocrellin derivative photosensitizer according to the invention has higher ability to photodynamically inactivate tumor cells than the first and second generation commercial photosensitizers.
Methods of manufacturing treprostinil and treprostinil derivative prodrugs
Methods for making prodrugs of treprostinil and treprostinil derivatives are provided. Specifically, methods are provided herein for producing prostacyclin compounds comprising treprostinil covalently linked to a linear C.sub.5-C.sub.18 alkyl, branched C.sub.5-C.sub.18 alkyl, linear C.sub.2-C.sub.18 alkenyl, branched C.sub.3-C.sub.18 alkenyl, aryl, aryl-C.sub.1-C.sub.18 alkyl or an amino acid or a peptide (e.g., dipeptide, tripeptide, tetrapeptide). The linkage, in one embodiment, is via an amide or ester bond. Prostacyclin compounds provided herein can also include at least one hydrogen atom substituted with at least one deuterium atom. The compounds provided herein can be used to treat pulmonary hypertension (e.g., pulmonary arterial hypertension) and portopulmonary hypertension.
CYCLOHEPTYLAMINE DERIVATIVES AS ANTI-DIABETIC AGENTS
Cycloalkylamine derivatives may be used for preventing or treating diseases in humans, animals, and have demonstrated efficacy specifically in treating type 2 diabetes. In an embodiment, the cycloalkylamine derivatives can include a compound selected from the group consisting of cycloheptanamine salts, cyclohexanamine salts, cyclopentanamine salts 1-cycloheptyl-[4,4′-bipyridin]-1-ium, N1,N2-dicycloheptyloxalamide, 1-[3′,5′-bis(trifluoromethyl)phenyl]-3-cycloheptylurea, 1,1′-(4-methyl-1,3-phenylene)bis(3-cycloheptylurea), 1-(2′-aminopyrimidin-4′-yl)-3-cycloheptylurea, 4-amino-N-(cycloheptylcarbamoyl)benzenesulfonamide, 4-(3′-cycloheptylureido)-N-(5″-methylisoxazol-3″-yl)benzenesulfonamide, N-(cycloheptylcarbamoyl)-4-methylbenzenesulfonamide, 1-cycloheptylguanidine hydrochloride, (E)-amino[(amino(cycloheptylamino)methylene)amino]methaniminium chloride, or a pharmaceutically acceptable salt thereof.
PROSTACYCLIN COMPOUNDS, COMPOSITIONS AND METHODS OF USE THEREOF
Prostacyclin compounds and compositions comprising the same are provided herein. Specifically, prostacyclin compounds comprising treprostinil covalently linked to a linear C.sub.5-C.sub.18 alkyl, branched C.sub.5-C.sub.18 alkyl, linear C.sub.2-C.sub.18 alkenyl, branched C.sub.3-C.sub.18 alkenyl, aryl, aryl-C.sub.1-C.sub.18 alkyl or an amino acid or a peptide (e.g., dipeptide, tripeptide, tetrapeptide) are described. The linkage, in one embodiment, is via a carbamate, amide or ester bond. Prostacyclin compounds provided herein can also include at least one hydrogen atom substituted with at least one deuterium atom. Methods for treating pulmonary hypertension (e.g., pulmonary arterial hypertension) and portopulmonary hypertension are also provided.
ENVIRONMENTALLY-FRIENDLY HYDROAZIDATION OF OLEFINS
The present invention provides processes for the synthesis of organic azides, intermediates for the production thereof, and compositions related thereto.
HEPATITIS B ANTIVIRAL AGENTS
The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof:
X-A-Y-L-R (I)
which inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV life cycle of the hepatitis B virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HBV infection. The invention also relates to methods of treating an HBV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
PERFLUOROAMINOOLEFINS AND METHODS OF MAKING AND USING THE SAME
Described herein is a perfluorinated aminoolefin compound of general formula (I): CFY═CXN(R.sub.f)CF.sub.2R.sub.f′ where: (a) R.sub.f and R.sub.f′ are (i) independently selected from a linear or branched perfluoroalkyl group having 1-8 carbon atoms, optionally comprising at least one catenated O or N atom, or (ii) bonded together to form a perfluorinated ring structure having 4-8 ring carbon atoms, optionally comprising at least one catenated O atom; and (b) X and Y are (i) independently selected from a perfluoroalkyl group having 1-4 carbon atoms, or (ii) bonded together to form a perfluorinated ring structure having 5-6 ring carbon atoms. Such compounds may be used in heat transfer, foam blowing or immersion cooling applications, or as a working fluid in a Rankine cycle, a coating or lubricant, or as a dielectric fluid. Also disclosed herein is a method for making such compounds.
Novel Glutamine Analogs
The invention relates to novel glutamine analogs, a composition containing the glutamine analogs and the use thereof.
PHENYL UREA DERIVATIVES AS N-FORMYL PEPTIDE RECEPTOR MODULATORS
The present invention relates to phenyl urea derivatives useful for the treatment of inflammatory diseases, pharmaceutical compositions containing them and their use as tools or as pharmaceuticals as modulators of the N-formyl peptide receptor (FPR), including FPR1 and FPR2, or as selective agonists of the FPR1 receptor.
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