Patent classifications
C07C35/37
LABELING METHOD, OXIDANT FOR LABELING, RUTHENIUM COMPLEX, CATALYST, LABELING COMPOUND, AND COMPOUND
Provided is a labeling method having a step of labeling a substrate having a carbon-hydrogen bond with an oxygen isotope by using a catalyst and an oxidant produced from a hypervalent iodine compound having an ester structure and labeled water labeled with at least one oxygen isotope selected from the group consisting of .sup.17O and .sup.18O. Also provided is an oxidant for labeling that is produced from a hypervalent iodine compound having an ester structure and labeled water labeled with at least one oxygen isotope selected from the group consisting of .sup.17O and .sup.18O and labels a substrate having a carbon-hydrogen bond with an oxygen isotope in the co-presence of a catalyst.
ALKYNES AND METHODS OF REACTING ALKYNES WITH 1,3-DIPOLE-FUNCTIONAL COMPOUNDS
1,3-Dipole-functional compounds (e.g., azide functional compounds) can be reacted with certain alkynes in a cyclization reaction to form heterocyclic compounds. Useful alkynes (e.g., strained, cyclic alkynes) and methods of making such alkynes are also disclosed. The reaction of 1,3-dipole-functional compounds with alkynes can be used for a wide variety of applications including the immobilization of biomolecules on a substrate.
ALKYNES AND METHODS OF REACTING ALKYNES WITH 1,3-DIPOLE-FUNCTIONAL COMPOUNDS
1,3-Dipole-functional compounds (e.g., azide functional compounds) can be reacted with certain alkynes in a cyclization reaction to form heterocyclic compounds. Useful alkynes (e.g., strained, cyclic alkynes) and methods of making such alkynes are also disclosed. The reaction of 1,3-dipole-functional compounds with alkynes can be used for a wide variety of applications including the immobilization of biomolecules on a substrate.
SMALL MOLECULE INHIBITORS OF NECROPTOSIS
The invention features a series of heterocyclic derivatives that inhibit tumor necrosis factor alpha (TNF-) induced necroptosis. The heterocyclic compounds of the invention are described by Formulas (I)-(VIII) and by Compounds (1)-(7), (13)-(26), (27)-(33), (48)-(57), and (58)-(70). These necrostatins are shown to inhibit TNF- induced necroptosis in FADD-deficient variant of human Jurkat T cells. The invention further features pharmaceutical compositions featuring necrostatins. The compounds and compositions of the invention may also be used to treat disorders where necroptosis is likely to play a substantial role.
SMALL MOLECULE INHIBITORS OF NECROPTOSIS
The invention features a series of heterocyclic derivatives that inhibit tumor necrosis factor alpha (TNF-) induced necroptosis. The heterocyclic compounds of the invention are described by Formulas (I)-(VIII) and by Compounds (1)-(7), (13)-(26), (27)-(33), (48)-(57), and (58)-(70). These necrostatins are shown to inhibit TNF- induced necroptosis in FADD-deficient variant of human Jurkat T cells. The invention further features pharmaceutical compositions featuring necrostatins. The compounds and compositions of the invention may also be used to treat disorders where necroptosis is likely to play a substantial role.
Strepsesquitriol, preparation method thereof, and application thereof
The invention discloses a new strepsesquitriol A, a preparation method thereof and an application thereof. Strepsesquitriol A, a structure as shown in Formula (I), is a compound having a new skeleton and strongly inhibiting the formation of LPS-induced TNF but showing no cytotoxic activity, so it can be used for the preparation of anti-inflammatory drug or act as a precursor of anti-inflammatory drugs, for the treatment of multiple inflammations. Therefore, the invention provides a new candidate compound for the development of anti-inflammatory drugs, and is of great significance for developing Chinese marine drug resources. ##STR00001##
Strepsesquitriol, preparation method thereof, and application thereof
The invention discloses a new strepsesquitriol A, a preparation method thereof and an application thereof. Strepsesquitriol A, a structure as shown in Formula (I), is a compound having a new skeleton and strongly inhibiting the formation of LPS-induced TNF but showing no cytotoxic activity, so it can be used for the preparation of anti-inflammatory drug or act as a precursor of anti-inflammatory drugs, for the treatment of multiple inflammations. Therefore, the invention provides a new candidate compound for the development of anti-inflammatory drugs, and is of great significance for developing Chinese marine drug resources. ##STR00001##
Small molecule inhibitors of necroptosis
Compounds having the following structure (VI-A): ##STR00001##
or any pharmaceutically acceptable salt or solvate thereof, or any stereoisomer thereof, wherein R.sub.E1, R.sub.E2, R.sub.E3, R.sub.E4, Z.sub.E2 and Z.sub.E3 are as disclosed herein, are provided. Pharmaceutical compositions comprising the compounds, and methods for use of the compounds for treating disorders associated with necrosptosis are also provided.
Small molecule inhibitors of necroptosis
Compounds having the following structure (VI-A): ##STR00001##
or any pharmaceutically acceptable salt or solvate thereof, or any stereoisomer thereof, wherein R.sub.E1, R.sub.E2, R.sub.E3, R.sub.E4, Z.sub.E2 and Z.sub.E3 are as disclosed herein, are provided. Pharmaceutical compositions comprising the compounds, and methods for use of the compounds for treating disorders associated with necrosptosis are also provided.
OXYGEN-ABSORBING COMPOUND, AND OXYGEN-ABSORBING ADHESIVE COMPOSITION AND OXYGEN-ABSORBING COATING AGENT COMPOSITION EACH USING SAME
An oxygen-absorbing compound has oxygen-absorbing properties and generates less odor. An oxygen-absorbing adhesive composition and a coating agent composition are produced using the oxygen-absorbing compound. The adhesive composition is used for forming an adhesive layer in a laminate for a packaging material, generates less odor, absorbs oxygen in a packaging bag or a packaging container to prevent the deterioration of a content in the packaging bag or the packaging container, and has an excellent balance among adhesion strength, the amount of generated odor and oxygen adsorption properties. The coating agent composition forms a coating layer for the surface of the laminate for a packaging material, generates less odor, and absorbs oxygen penetrating through the laminate or oxygen in a packaging bag or container. The oxygen-absorbing compound has one or two or more unsaturated five-membered rings that have a carbon-carbon double bond.