Patent classifications
C07D313/14
HIGH PENETRATION COMPOSITIONS AND THEIR APPLICATIONS
The invention provides compositions or pharmaceutical compositions of novel high penetration compositions (HPC) of a parent compound, which are capable of crossing biological barriers with high penetration efficiency. The HPCs are capable of being converted to parent drugs or parent drug-related compounds such as metabolites after crossing one or more biological barriers and thus can render treatments for the conditions that the parent drugs or parent drug-related compounds can. Additionally, the HPCs are capable of reaching areas that their parent drugs or parent drug-related compounds may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. For example, HPCs of NSAIA have demonstrated indications such as treating hair loss and bold. A HPC can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.
HIGH PENETRATION COMPOSITIONS AND THEIR APPLICATIONS
The invention provides compositions or pharmaceutical compositions of novel high penetration compositions (HPC) of a parent compound, which are capable of crossing biological barriers with high penetration efficiency. The HPCs are capable of being converted to parent drugs or parent drug-related compounds such as metabolites after crossing one or more biological barriers and thus can render treatments for the conditions that the parent drugs or parent drug-related compounds can. Additionally, the HPCs are capable of reaching areas that their parent drugs or parent drug-related compounds may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. For example, HPCs of NSAIA have demonstrated indications such as treating hair loss and bold. A HPC can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.
Compound and polymer compound containing the compound
Provided is a compound having higher fluorescence quantum yield and higher optical stability than a conventional FLAP and a polymer compound containing the compound. ##STR00001## A: seven or eight-membered ring structure, Y.sup.1, Y.sup.2, Y.sup.3: halogen atom or the like, a1: number of Y.sup.1, a2: number of Y.sup.2, B: number of Y.sup.3, 0≤m and n≤3: when 1≤m≤3, Y.sup.1 may be substituted with a structure portion defined by m, when 1≤n≤3, Y.sup.2 may be substituted with a structure portion defined by n, and B.sup.1, B.sup.2: Formulas (2-1) to (2-3). ##STR00002## C.sup.1, C.sup.2, C.sup.3: structure containing a cyclic hydrocarbon compound, D.sup.1, D.sup.2, D.sup.3: substructure that inhibits aggregation, E.sup.1, E.sup.2, E.sup.3: polymerizable substructure, Z.sup.1: hydrogen atom or the like, c: number of substituent groups Z.sup.1, Z.sup.2, Z.sup.3: hydrogen atom or the like, and may form a ring with C.sup.2.
Compound and polymer compound containing the compound
Provided is a compound having higher fluorescence quantum yield and higher optical stability than a conventional FLAP and a polymer compound containing the compound. ##STR00001## A: seven or eight-membered ring structure, Y.sup.1, Y.sup.2, Y.sup.3: halogen atom or the like, a1: number of Y.sup.1, a2: number of Y.sup.2, B: number of Y.sup.3, 0≤m and n≤3: when 1≤m≤3, Y.sup.1 may be substituted with a structure portion defined by m, when 1≤n≤3, Y.sup.2 may be substituted with a structure portion defined by n, and B.sup.1, B.sup.2: Formulas (2-1) to (2-3). ##STR00002## C.sup.1, C.sup.2, C.sup.3: structure containing a cyclic hydrocarbon compound, D.sup.1, D.sup.2, D.sup.3: substructure that inhibits aggregation, E.sup.1, E.sup.2, E.sup.3: polymerizable substructure, Z.sup.1: hydrogen atom or the like, c: number of substituent groups Z.sup.1, Z.sup.2, Z.sup.3: hydrogen atom or the like, and may form a ring with C.sup.2.
High penetration compositions and their applications
High penetration compositions (HPC) of a parent compound, which are capable of crossing biological barriers with high penetration efficiency. The HPCs are capable of being converted to parent drugs or parent drug-related compounds such as metabolites after crossing one or more biological barriers and thus can render treatments for the conditions that the parent drugs or parent drug-related compounds can. Additionally, the HPCs are capable of reaching areas that their parent drugs or parent drug-related compounds may not be able to access or to render a sufficient concentration at the target areas HPCs of NSAIA, for example, have demonstrated indications such as treating hair loss. A HPC can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.
High penetration compositions and their applications
High penetration compositions (HPC) of a parent compound, which are capable of crossing biological barriers with high penetration efficiency. The HPCs are capable of being converted to parent drugs or parent drug-related compounds such as metabolites after crossing one or more biological barriers and thus can render treatments for the conditions that the parent drugs or parent drug-related compounds can. Additionally, the HPCs are capable of reaching areas that their parent drugs or parent drug-related compounds may not be able to access or to render a sufficient concentration at the target areas HPCs of NSAIA, for example, have demonstrated indications such as treating hair loss. A HPC can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.
PHOTOACTIVE FLUOROPHORES AND METHODS OF IN VIVO LABELING
Provided are a photoactive fluorophore, a photoactive ligand, and a photoactive complex. The photoactive fluorophore includes a photoactivatable derivative of an azetidine-containing Janelia-Fluor dye. The photoactive ligand includes a photoactive fluorophore and a protein tag. The photoactive complex includes a photoactive ligand conjugated to a protein. Also provided are methods of in vivo labeling with and photoactivation of the photoactive fluorophore, ligand, and complex.
PHOTOACTIVE FLUOROPHORES AND METHODS OF IN VIVO LABELING
Provided are a photoactive fluorophore, a photoactive ligand, and a photoactive complex. The photoactive fluorophore includes a photoactivatable derivative of an azetidine-containing Janelia-Fluor dye. The photoactive ligand includes a photoactive fluorophore and a protein tag. The photoactive complex includes a photoactive ligand conjugated to a protein. Also provided are methods of in vivo labeling with and photoactivation of the photoactive fluorophore, ligand, and complex.
COMPOUND AND POLYMER COMPOUND CONTAINING THE COMPOUND
Provided is a compound having higher fluorescence quantum yield and higher optical stability than a conventional FLAP and a polymer compound containing the compound.
##STR00001## A: seven or eight-membered ring structure, Y.sup.1, Y.sup.2, Y.sup.3: halogen atom or the like, al: number of Y.sup.1, a2: number of Y.sup.2, B: number of Y.sup.3, 0≤m and n≤3: when 1≤m≤3, Y.sup.1 may be substituted with a structure portion defined by m, when 1≤n≤3, Y.sup.2 may be substituted with a structure portion defined by n, and B.sup.1, B.sup.2: Formulas (2-1) to (2-3):
##STR00002## C.sup.1, C.sup.2, C.sup.3: structure containing a cyclic hydrocarbon compound, D.sup.1, D.sup.2, D.sup.3: substructure that inhibits aggregation, E.sup.1, E.sup.2, E.sup.3: polymerizable substructure, Z.sup.1: hydrogen atom or the like, c: number of substituent groups Z.sup.1, Z.sup.2, Z.sup.3: hydrogen atom or the like, and may form a ring with C.sup.2.
COMPOUND AND POLYMER COMPOUND CONTAINING THE COMPOUND
Provided is a compound having higher fluorescence quantum yield and higher optical stability than a conventional FLAP and a polymer compound containing the compound.
##STR00001## A: seven or eight-membered ring structure, Y.sup.1, Y.sup.2, Y.sup.3: halogen atom or the like, al: number of Y.sup.1, a2: number of Y.sup.2, B: number of Y.sup.3, 0≤m and n≤3: when 1≤m≤3, Y.sup.1 may be substituted with a structure portion defined by m, when 1≤n≤3, Y.sup.2 may be substituted with a structure portion defined by n, and B.sup.1, B.sup.2: Formulas (2-1) to (2-3):
##STR00002## C.sup.1, C.sup.2, C.sup.3: structure containing a cyclic hydrocarbon compound, D.sup.1, D.sup.2, D.sup.3: substructure that inhibits aggregation, E.sup.1, E.sup.2, E.sup.3: polymerizable substructure, Z.sup.1: hydrogen atom or the like, c: number of substituent groups Z.sup.1, Z.sup.2, Z.sup.3: hydrogen atom or the like, and may form a ring with C.sup.2.