Patent classifications
A61K47/65
ASYMMETRICALLY BRANCHED DEGRADABLE POLYETHYLENE GLYCOL DERIVATIVE
A branched degradable polyethylene glycol derivative with a high molecular weight that does not cause vacuolation of cells is provided. A branched degradable polyethylene glycol derivative represented by the following formula (1), containing, in a molecule, an oligopeptide that is degraded in the cells:
##STR00001##
wherein k.sub.1 and k.sub.2 are each independently 1-12, j.sub.1 and j.sub.2 are each independently 45-950, R is a hydrogen atom, a substituted or unsubstituted alkyl group having 1-12 carbon atoms, a substituted aryl group, an aralkyl group or a heteroalkyl group, Z is an oligopeptide that is degraded by enzyme in the cells, X is a functional group capable of reacting with a bio-related substance, and L.sub.1 and L.sub.2 are each independently a single bond or a divalent spacer.
Anti-tumor compound and preparation method and use thereof
The present application relates to an anti-tumor compound and a preparation method and use thereof, and in particular to a compound or a tautomer, a mesomer, a racemate, an enantiomer or a diastereoisomer thereof, or a mixture thereof, or a pharmaceutically acceptable salt thereof, and a preparation method and use thereof.
Anti-tumor compound and preparation method and use thereof
The present application relates to an anti-tumor compound and a preparation method and use thereof, and in particular to a compound or a tautomer, a mesomer, a racemate, an enantiomer or a diastereoisomer thereof, or a mixture thereof, or a pharmaceutically acceptable salt thereof, and a preparation method and use thereof.
Therapeutic molecules
The present invention relates to effective pain therapies in companion animals. In particular, an isolated companion animal p75NTR protein or a fusion protein containing the same or portions thereof are contemplated. Nucleic acids encoding the proteins are also encompassed in the invention as well as methods of using the same.
Therapeutic molecules
The present invention relates to effective pain therapies in companion animals. In particular, an isolated companion animal p75NTR protein or a fusion protein containing the same or portions thereof are contemplated. Nucleic acids encoding the proteins are also encompassed in the invention as well as methods of using the same.
MCL-1 INHIBITOR ANTIBODY-DRUG CONJUGATES AND METHODS OF USE
- Matthew T. Burger ,
- Maia Chanrion ,
- Frédéric COLLAND ,
- Marton Csekei ,
- Lea Delacour ,
- Patrice Desos ,
- Olivier Geneste ,
- Jean-Michel Henlin ,
- Vesela KOSTOVA ,
- Andras Kotschy ,
- Ana Leticia Maragno ,
- Eric MCNEILL ,
- Mark G. Palermo ,
- Francesca Rocchetti ,
- Jérôme Starck ,
- Bing YU ,
- Qiang Zhang ,
- Ágnes Proszenyák ,
- Szabolcs Sipos ,
- Zhuoliang Chen ,
- Katsumasa NAKAJIMA ,
- Joseph Anthony D'ALESSIO ,
- John William Blankenship
Anti-CD74 antibody-drug conjugates are disclosed. The anti-CD74 antibody-drug conjugates comprise an Mcl-1 inhibitor drug moiety and an anti-CD74 antibody or antigen-binding fragment thereof that binds an antigen target, e.g., an antigen expressed on a tumor or other cancer cell. The disclosure further relates to methods and compositions for use in the treatment of cancers by administering the antibody-drug conjugates provided herein. Linker-drug conjugates comprising an Mcl-1 inhibitor drug moiety and methods of making same are also disclosed.
UNSATURATED FATTY ACID-CONJUGATED CP2C-TARGETING PEPTIDE-BASED ANTICANCER AGENT
The present invention relates to an unsaturated fatty acid-conjugated CP2c-targeting peptide-based agent. In the present invention, it was confirmed that by linking an unsaturated fatty acid to ACP52C, which is a CP2c-targeting peptide lead substance exhibiting an effect as a general-purpose anticancer agent, in vivo stability was improved without affecting the anticancer effect. Further, cancer cell-specific anticancer efficacy was confirmed in various cancer cells and normal cells.
UNSATURATED FATTY ACID-CONJUGATED CP2C-TARGETING PEPTIDE-BASED ANTICANCER AGENT
The present invention relates to an unsaturated fatty acid-conjugated CP2c-targeting peptide-based agent. In the present invention, it was confirmed that by linking an unsaturated fatty acid to ACP52C, which is a CP2c-targeting peptide lead substance exhibiting an effect as a general-purpose anticancer agent, in vivo stability was improved without affecting the anticancer effect. Further, cancer cell-specific anticancer efficacy was confirmed in various cancer cells and normal cells.
Antibody-drug conjugates with high drug loading
The present invention provides transglutaminase-mediated antibody-drug conjugates with high anti-body-drug ratio (DAR) comprising 1) glutamine-containing tags, endogenous glutamines, and/or endogenous glutamines made reactive by antibody engineering or an engineered transglutaminase (e.g., with altered substrate specifity); and 2) amine donor agents comprising amine donor units, linkers, and agent moieties, wherein the DAR is at least about 5. The invention also provides methods of making and methods of using such higher drug loaded antibody-drug conjugates.
Antibody-drug conjugates with high drug loading
The present invention provides transglutaminase-mediated antibody-drug conjugates with high anti-body-drug ratio (DAR) comprising 1) glutamine-containing tags, endogenous glutamines, and/or endogenous glutamines made reactive by antibody engineering or an engineered transglutaminase (e.g., with altered substrate specifity); and 2) amine donor agents comprising amine donor units, linkers, and agent moieties, wherein the DAR is at least about 5. The invention also provides methods of making and methods of using such higher drug loaded antibody-drug conjugates.