Patent classifications
C07D498/18
HETEROCYCLIC DERIVATIVES, PHARMACEUTICAL COMPOSITIONS AND THEIR USE IN THE TREATMENT, AMELIORATION OR PREVENTION OF CANCER
The present invention relates to a compound of formula (I), optionally in the form of a pharmaceutically acceptable salt, solvate, cocrystal, tautomer, racemate, enantiomer, or diastereomer or mixture thereof Formula (I) and to pharmaceutical compositions comprising a compound of formula (I), as well as to the use of a compound of formula (I), or a pharmaceutically acceptable salt, solvate, cocrystal, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, in the treatment of cancer. Further aspects of the present invention include combination therapies in which a compound of formula (I), as well as to the use of a compound of formula (I), or a pharmaceutically acceptable salt, solvate, cocrystal, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, is used in combination with a known anti-cancer agent.
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HETEROCYCLIC DERIVATIVES, PHARMACEUTICAL COMPOSITIONS AND THEIR USE IN THE TREATMENT, AMELIORATION OR PREVENTION OF CANCER
The present invention relates to a compound of formula (I), optionally in the form of a pharmaceutically acceptable salt, solvate, cocrystal, tautomer, racemate, enantiomer, or diastereomer or mixture thereof Formula (I) and to pharmaceutical compositions comprising a compound of formula (I), as well as to the use of a compound of formula (I), or a pharmaceutically acceptable salt, solvate, cocrystal, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, in the treatment of cancer. Further aspects of the present invention include combination therapies in which a compound of formula (I), as well as to the use of a compound of formula (I), or a pharmaceutically acceptable salt, solvate, cocrystal, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, is used in combination with a known anti-cancer agent.
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IMMUNOPHILIN BINDING AGENTS AND USES THEREOF
Described herein, inter alia, are immunophilin binding compounds and methods of heating CNS diseases, including co-administering outside the CNS of a subject an anti-CNS disease drug and a compound described herein.
Antimicrobial Compounds and Methods
The invention is directed to compounds that are active as antibacterial agents. The invention compounds are active against gram-positive and gram-negative bacteria and can be used to treat infections caused by gram-positive and gram-negative bacteria. Also disclosed are processes and intermediates for making the compounds.
Antimicrobial Compounds and Methods
The invention is directed to compounds that are active as antibacterial agents. The invention compounds are active against gram-positive and gram-negative bacteria and can be used to treat infections caused by gram-positive and gram-negative bacteria. Also disclosed are processes and intermediates for making the compounds.
SITE-SPECIFIC ANTIBODY CONJUGATION AND ANTIBODY-DRUG CONJUGATE AS SPECIFIC EMBODIMENT THEREOF
The present invention relates to technology capable of labeling a certain site of an antibody with a certain number of chemical functional groups or cargo moieties. The present invention may provide an antibody product having high uniformity. The present invention may provide an antibody product whose antibody functions are not degraded. That is, the present invention may provide an antibody product whose antibody binding affinity and half-life are not degraded. The present invention is of great significance as being the first technology allowing site-specific labeling of an antibody without any complicated processes.
COMPOUND AND LABELED BIOLOGICAL SUBSTANCE USING THE SAME
There are provided a compound of Formula (1) and a labeled biological substance having the compound.
##STR00001##
R.sup.1 to R.sup.6, R.sup.11 to R.sup.13, and R.sup.22 to R.sup.29 represent specific groups, and n is an integer of 1 to 3.
One selected from R.sup.1, R.sup.2, R.sup.5, R.sup.22 to R.sup.25 and one selected from R.sup.3, R.sup.4, R.sup.6, and R.sup.26 to R.sup.29 are bonded through a linking group LL.
The linking group LL represents a linking group having 1 to 100 atoms, which does not have any one of an aromatic hydrocarbon ring, a sulfo group, or a phosphono group.
R.sup.1, . . . , R.sup.6, R.sup.22, . . . , or R.sup.29 includes a structure represented by —(CH.sub.2—CH.sub.2—O).sub.m—, where m is 1 to 50.
The above-described compound is a neutral compound and contains at least one substituent capable of being bonded to a carboxy group or a biological substance.
FUSED TETRACYCLIC QUINAZOLINE DERIVATIVES AS INHIBITORS OF ERBB2
The present disclosure relates generally to compounds and compositions thereof for inhibition of ErbB2, including mutant forms of ErbB2, particularly those harboring an Exon 20 mutation, methods of preparing said compounds and compositions, and their use in the treatment or prophylaxis of various cancers, such as lung, glioma, skin, head neck, salivary gland, breast, esophageal, liver, stomach (gastric), uterine, cervical, biliary tract, pancreatic, colorectal, renal, bladder or prostate cancer.
FUSED TETRACYCLIC QUINAZOLINE DERIVATIVES AS INHIBITORS OF ERBB2
The present disclosure relates generally to compounds and compositions thereof for inhibition of ErbB2, including mutant forms of ErbB2, particularly those harboring an Exon 20 mutation, methods of preparing said compounds and compositions, and their use in the treatment or prophylaxis of various cancers, such as lung, glioma, skin, head neck, salivary gland, breast, esophageal, liver, stomach (gastric), uterine, cervical, biliary tract, pancreatic, colorectal, renal, bladder or prostate cancer.
MAYTANSINOID DERIVATIVES, CONJUGATES THEREOF, AND METHODS OF USE
Provided herein are maytansinoid compounds, derivatives thereof, conjugates thereof, and methods of treating or preventing proliferative diseases with the same.