Patent classifications
C07D207/456
REVERSIBLE COVALENT LINKAGE OF FUNCTIONAL MOLECULES
The present invention relates to the use of a compound containing a moiety of formula (I) as a reagent for linking a compound of formula R.sub.1-H which comprises a first functional moiety of formula F.sub.1 to a second functional moiety of formula F.sub.2
##STR00001##
wherein X, X, Y, R.sub.1, F.sub.1 and F.sub.2 are as defined herein. The present invention also provides related processes and products. The present invention is useful for creating functional conjugate compounds, and specifically conjugates in which at least one of the constituent molecules carries a thiol group.
REVERSIBLE COVALENT LINKAGE OF FUNCTIONAL MOLECULES
The present invention relates to the use of a compound containing a moiety of formula (I) as a reagent for linking a compound of formula R.sub.1-H which comprises a first functional moiety of formula F.sub.1 to a second functional moiety of formula F.sub.2
##STR00001##
wherein X, X, Y, R.sub.1, F.sub.1 and F.sub.2 are as defined herein. The present invention also provides related processes and products. The present invention is useful for creating functional conjugate compounds, and specifically conjugates in which at least one of the constituent molecules carries a thiol group.
CURABLE COMPOUND
There is provided a curable compound having good solvent solubility and being capable of forming a cured material having super heat resistance. The curable compound according to the present invention is represented by the following formula (1). In the formula (1), R.sup.1 and R.sup.2 each represent a curable functional group; D.sup.1 and D.sup.2 each represent a single bond or a linking group; and L represents a divalent group having a repeating unit containing a structure represented by the following formula (I) and a structure represented by the following formula (II) (wherein Ar.sup.1 to Ar.sup.3 each represent a group made by eliminating two hydrogen atoms from a structural formula of an aromatic ring or a group made by eliminating two hydrogen atoms from a structural formula in which two or more aromatic rings are bound through a single bond or a linking group; X represents CO, S or SO.sub.2; each Y represents S, SO.sub.2, O, CO, COO or CONH; and n represents an integer of 0 or more):
##STR00001##
TYPE III DEIODINASE INHIBITORS AND USES THEREOF
The present invention relates to compounds that inhibit the activity of Type III deiodinase (DIO3). The present invention further relates to methods for treating or preventing depression, depression associated with other psychiatric or general medical diseases or conditions, condition amenable to treatment with known anti-depressants and cancer, particularly by using the compounds of the invention.
TYPE III DEIODINASE INHIBITORS AND USES THEREOF
The present invention relates to compounds that inhibit the activity of Type III deiodinase (DIO3). The present invention further relates to methods for treating or preventing depression, depression associated with other psychiatric or general medical diseases or conditions, condition amenable to treatment with known anti-depressants and cancer, particularly by using the compounds of the invention.
DI-SUBSTITUTED MALEIC AMIDE LINKER FOR ANTIBODY-DRUG CONJUGATING AND PREPARATION METHOD AND USE THEREOF
Provided in the present invention are a di-substituted maleic amide linker conjugated to an antibody and a preparation method and use thereof. In particular, the present invention conjugates a strongly cytotoxic active substance to a biomacromolecule through a class of new linkers. The class of linkers can selectively act simultaneously with disulphide chains, so as to greatly improve the substance homogeneity of a conjugate. The conjugate prepared by the linker of the present invention has a high inhibitory activity on a cell strain expressing the corresponding antigen. Also provided is a method for preparing the above-mentioned conjugate and the use.
DI-SUBSTITUTED MALEIC AMIDE LINKER FOR ANTIBODY-DRUG CONJUGATING AND PREPARATION METHOD AND USE THEREOF
Provided in the present invention are a di-substituted maleic amide linker conjugated to an antibody and a preparation method and use thereof. In particular, the present invention conjugates a strongly cytotoxic active substance to a biomacromolecule through a class of new linkers. The class of linkers can selectively act simultaneously with disulphide chains, so as to greatly improve the substance homogeneity of a conjugate. The conjugate prepared by the linker of the present invention has a high inhibitory activity on a cell strain expressing the corresponding antigen. Also provided is a method for preparing the above-mentioned conjugate and the use.
NOVEL ANTIBODY-DRUG CONJUGATES AND THE USE OF SAME IN THERAPY
Disclosed are novel antibody-drug conjugates and use thereof in therapy, in particular in anticancer or anti-inflammatory therapy, as well as synthetic products useful as linkers, composed of a linker head and a linker body, and also a method for preparing the linkers and the antibody-drug conjugates.
NOVEL ANTIBODY-DRUG CONJUGATES AND THE USE OF SAME IN THERAPY
Disclosed are novel antibody-drug conjugates and use thereof in therapy, in particular in anticancer or anti-inflammatory therapy, as well as synthetic products useful as linkers, composed of a linker head and a linker body, and also a method for preparing the linkers and the antibody-drug conjugates.
Type III deiodinase inhibitors and uses thereof
The present invention relates to compounds that inhibit the activity of Type III deiodinase (DIO3). The present invention further relates to methods for treating or preventing depression, depression associated with other psychiatric or general medical diseases or conditions, condition amenable to treatment with known anti-depressants and cancer, particularly by using the compounds of the invention.