Patent classifications
C07D249/16
PHOTOCURABLE COMPOSITION
A photocurable composition can comprising a polymerizable material, a hindered stabilizer, and a photoinitiator, wherein the polymerizable material comprises at least one multi-functional aromatic vinyl monomer; and the hindered stabilizer is a hindered amine of formula (1) or a hindered phenol of formula (2)
##STR00001##
wherein X is H, CH.sub.3, or YZ; Y is CH.sub.2, O, S, or N; Z is an organic substituent; R.sub.1 is H, CH.sub.3, OH, OR.sub.5, COCH.sub.3, or C(?O)R.sub.5; R.sub.2, R.sub.3, R.sub.4, R.sub.5 is an organic substituent.
PHOTOCURABLE COMPOSITION
A photocurable composition can comprising a polymerizable material, a hindered stabilizer, and a photoinitiator, wherein the polymerizable material comprises at least one multi-functional aromatic vinyl monomer; and the hindered stabilizer is a hindered amine of formula (1) or a hindered phenol of formula (2)
##STR00001##
wherein X is H, CH.sub.3, or YZ; Y is CH.sub.2, O, S, or N; Z is an organic substituent; R.sub.1 is H, CH.sub.3, OH, OR.sub.5, COCH.sub.3, or C(?O)R.sub.5; R.sub.2, R.sub.3, R.sub.4, R.sub.5 is an organic substituent.
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.
Pretargeting kit for imaging or therapy comprising a trans-cyclooctene dienophile and a diene
Described is a pretargeting method, and related kits, for targeted medical imaging and/or therapeutics, wherein use is made of abiotic reactive chemical groups that exhibit bio-orthogonal reactivity towards each other. The invention involves the use of [4+2] inverse electron demand (retro) Diels-Alder chemistry in providing the coupling between a Pre-targeting Probe and an Effector Probe. To this end one of these probes comprises an electron-deficient tetrazine or other suitable diene, and the other an E-cyclooctene which has a flattened structure as a result of the position of at least two exocyclic bonds.
Pretargeting kit for imaging or therapy comprising a trans-cyclooctene dienophile and a diene
Described is a pretargeting method, and related kits, for targeted medical imaging and/or therapeutics, wherein use is made of abiotic reactive chemical groups that exhibit bio-orthogonal reactivity towards each other. The invention involves the use of [4+2] inverse electron demand (retro) Diels-Alder chemistry in providing the coupling between a Pre-targeting Probe and an Effector Probe. To this end one of these probes comprises an electron-deficient tetrazine or other suitable diene, and the other an E-cyclooctene which has a flattened structure as a result of the position of at least two exocyclic bonds.
Crystalline form of (S)-(2-(6-chloro-7-methyl-1H-benzo[D]imidazol-2-yl)-2-methylpyrrolidin-1-yl)(5-methoxy-2-(2H-1,2,3-triazol-2-yl)phenyl)methanone and its use as orexin receptor antagonists
The invention relates to crystalline forms of (S)-(2-(6-chloro-7-methyl-1H-benzo[d]imidazol-2-yl)-2-methylpyrrolidin-1-yl)(5-methoxy-2-(2H-1,2,3-triazol-2-yl)phenyl)methanone, processes for the preparation thereof, pharmaceutical compositions containing such crystalline forms, pharmaceutical compositions prepared from such crystalline forms, and their use as a medicament, especially as orexin receptor antagonists.
Vinylogous thioester compounds and methods of use
Provided herein are vinylogous thioester compounds and methods for using the compounds.
Fused cyclooctyne compounds and their use in metal-free click reactions
The invention relates to fused cyclooctyne compounds, and to a method for their preparation. The invention also relates to a conjugate wherein a fused cyclooctyne compound according to the invention is conjugated to a label, and to the use of these conjugates in bioorthogonal labeling, imaging and/or modification, such as for example surface modification, of a target molecule. The invention further relates to a method for the modification of a target molecule, wherein a conjugate according to the invention is reacted with a compound comprising a 1,3-dipole or a 1,3-(hetero)diene.
Bis-octahydrophenanthrene carboxamide derivatives and protein conjugates thereof for use as LXR agonists
Provided herein are compounds or payloads, linker-payloads, antibody-drug conjugates, and compositions, and methods for the treatment of diseases and disorders associated with the liver X receptor, including bis-octahydrophenanthrene carboxamides and protein (e.g., antibody) drug conjugates thereof.