Patent classifications
C07D295/15
C-Met Modulators and Methods of Use
The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate and/or modulate kinase receptor, particularly c-Met, KDR, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.
AROMATIC COMPOUND, PREPARATION METHOD THEREFOR AND USE THEREOF IN DRUG
Disclosed is an aromatic compound. Such compounds can locally produce a long-lasting nerve blocking effect, have an analgesic effect, an anti-pruritic effect, etc., and can be used in the preparation of a long-acting local anaesthetic drug, a local analgesic drug and an anti-pruritic drug.
1-aryl-1-hydroxy-2,3-diamino-propyl amines, 1-heteroaryl-1-hydroxy-2,3-diamino-propyl amines and related compounds having analgesic and/or immuno stimulant activity
Compounds of the formula ##STR00001##
where the variables have the meaning defined in the specification have analgesic and/or immunostimulant effect in mammals.
1-aryl-1-hydroxy-2,3-diamino-propyl amines, 1-heteroaryl-1-hydroxy-2,3-diamino-propyl amines and related compounds having analgesic and/or immuno stimulant activity
Compounds of the formula ##STR00001##
where the variables have the meaning defined in the specification have analgesic and/or immunostimulant effect in mammals.
SEMI-SYNTHESIS PROCEDURES
Provided herein are improved processes for convening C7-amino-substituted tetracylines to C7-fluoro-substituted tetracyclines as well as intermediates produced by or used in these processes. In one embodiment, a thermal fluorination method is provided in which a suspension comprising a non-polar organic solvent and a C7-diazo-substituted tetracycline hexafluorophosphate, hexafluoarsenate or hexafluorosilicate salt, or a salt, solvate or combination thereof is healed to provide a C7-fluoro-substituted tetracyline, or salt, solvate or combination thereof. In another embodiment, a photolytic fluorination is provided in which a solution comprising an ionic liquid and a C-7diazo-substituted tetracyline tetrafluoroborate, hexafluorophosphate, hexafluoroarsenate or hexafluorosilicate salt, or a salt, solvate or combination thereof is irradiated to provide a C7-fluoro-substituted tetracyline, or salt, solvate or combination thereof.
SEMI-SYNTHESIS PROCEDURES
Provided herein are improved processes for convening C7-amino-substituted tetracylines to C7-fluoro-substituted tetracyclines as well as intermediates produced by or used in these processes. In one embodiment, a thermal fluorination method is provided in which a suspension comprising a non-polar organic solvent and a C7-diazo-substituted tetracycline hexafluorophosphate, hexafluoarsenate or hexafluorosilicate salt, or a salt, solvate or combination thereof is healed to provide a C7-fluoro-substituted tetracyline, or salt, solvate or combination thereof. In another embodiment, a photolytic fluorination is provided in which a solution comprising an ionic liquid and a C-7diazo-substituted tetracyline tetrafluoroborate, hexafluorophosphate, hexafluoroarsenate or hexafluorosilicate salt, or a salt, solvate or combination thereof is irradiated to provide a C7-fluoro-substituted tetracyline, or salt, solvate or combination thereof.
COMPOSITIONS AND METHODS FOR DELIVERING PHARMACEUTICALLY ACTIVE AGENTS
The invention relates to modified lysines of the formula (I). The invention further relates to polypeptides comprising one or more modified lysine residues, pharmaceutical delivery systems comprising these polypeptides, pharmaceutical compositions containing them, and to their use in therapy.
##STR00001##
COMPOSITIONS AND METHODS FOR DELIVERING PHARMACEUTICALLY ACTIVE AGENTS
The invention relates to modified lysines of the formula (I). The invention further relates to polypeptides comprising one or more modified lysine residues, pharmaceutical delivery systems comprising these polypeptides, pharmaceutical compositions containing them, and to their use in therapy.
##STR00001##
Modified Conjugated Diene-based Polymer And Method Of Preparing The Same
The present invention relates to a modifier represented by Formula 1, a method of preparing the same, a modified conjugated diene-based polymer having a high modification ratio which includes a modifier-derived functional group, and a method of preparing the polymer.
Modified Conjugated Diene-based Polymer And Method Of Preparing The Same
The present invention relates to a modifier represented by Formula 1, a method of preparing the same, a modified conjugated diene-based polymer having a high modification ratio which includes a modifier-derived functional group, and a method of preparing the polymer.