C07D209/60

Branched Discrete PEG Constructs

Disclosed are general and “substantially pure” branched discrete polyethylene glycol constructs useful in attaching to a variety of biologically active groups, for example, preferential locators, as well as biologics like enzymes, for use in diagnostics, e.g. imaging, therapeutics, theranostics, and moieties specific for other applications. In its simplest intermediate state, a branched discrete polyethylene glycol construct is terminated at one end by a chemically reactive moiety, “A”, a group that is reactive with a biologic material that creates “A”, which is a biologically reactive group, connected through custom-character to a branched core (BC) which has attached at least two dPEG-containing chains, indicated by the solid line, custom-character, having terminal groups, which can be charged, non-reactive or reactable moieties and containing between about 2 and 64 dPEG residues.

Detection method and detection probe for colibactin and colibactin-producing bacteria

The present invention provides a method and probe for determining colibactin and a colibactin-producing bacterium. According to the present invention, there is provided a fluorescent probe for detecting myristoyl asparagine using, for example, a tissue sample and a fecal sample and detecting enzyme activity of ClbP.

Cyanine dye compound and preparation method therefor, and dual-function agent for photodynamic therapy and preparation method therefor

Disclosed are a cyanine dye compound and a preparation method therefor, and a dual-function agent for photodynamic therapy and a preparation method therefor. The provided cyanine dye compound is connected to multiple markers, which improves the accuracy of combination of dye and tumor cells, effectively reduces the background value, and avoids excessive residues in the liver. The provided cyanine dye compound is conjugated with the photosensitizer at 2′″ position, so that tumor highly absorbs the conjugates.

Cyanine dye compound and preparation method therefor, and dual-function agent for photodynamic therapy and preparation method therefor

Disclosed are a cyanine dye compound and a preparation method therefor, and a dual-function agent for photodynamic therapy and a preparation method therefor. The provided cyanine dye compound is connected to multiple markers, which improves the accuracy of combination of dye and tumor cells, effectively reduces the background value, and avoids excessive residues in the liver. The provided cyanine dye compound is conjugated with the photosensitizer at 2′″ position, so that tumor highly absorbs the conjugates.

SYNTHETIC PROCESS

The invention generally relates to a process for preparing compounds, including Compound of Formula (I), useful as key intermediates in the preparation of compounds having RORγt antagonist properties.

##STR00001##

SYNTHETIC PROCESS

The invention generally relates to a process for preparing compounds, including Compound of Formula (I), useful as key intermediates in the preparation of compounds having RORγt antagonist properties.

##STR00001##

NEW TRICYCLIC 5-HT2 ANTAGONISTS
20220267268 · 2022-08-25 ·

The present invention relates to tricyclic 1-amidino-4-methyl-[2,3 fused]-2-pyrroline derivatives of the general formula (I). The invention specifically relates to such derivatives which exhibit antagonizing activity towards serotonin 5-HT.sub.2B receptors. The present invention also relates to use of said compounds as a medicament and for the treatment of fibrosis, cardiovascular diseases, pain, IBD, inflammatory diseases, and cancer, as well as pharmaceutical compositions comprising one or more of said compounds and methods of treatment.

##STR00001##

NEW TRICYCLIC 5-HT2 ANTAGONISTS
20220267268 · 2022-08-25 ·

The present invention relates to tricyclic 1-amidino-4-methyl-[2,3 fused]-2-pyrroline derivatives of the general formula (I). The invention specifically relates to such derivatives which exhibit antagonizing activity towards serotonin 5-HT.sub.2B receptors. The present invention also relates to use of said compounds as a medicament and for the treatment of fibrosis, cardiovascular diseases, pain, IBD, inflammatory diseases, and cancer, as well as pharmaceutical compositions comprising one or more of said compounds and methods of treatment.

##STR00001##

CC-1065 analogs and their conjugates

This invention relates to novel analogs of the DNA-alkylating agent CC-1065 and to their conjugates. Furthermore this invention concerns intermediates for the preparation of said agents and conjugates. The conjugates are designed to release their (multiple) payload after one or more activation steps and/or at a rate and time span controlled by the conjugate in order to selectively deliver and/or controllably release one or more of said DNA alkylating agents. The agents, conjugates, and intermediates can be used to treat an illness that is characterized by undesired (cell) proliferation. As an example, the agents and the conjugates of this invention may be used to treat a tumor.

CC-1065 analogs and their conjugates

This invention relates to novel analogs of the DNA-alkylating agent CC-1065 and to their conjugates. Furthermore this invention concerns intermediates for the preparation of said agents and conjugates. The conjugates are designed to release their (multiple) payload after one or more activation steps and/or at a rate and time span controlled by the conjugate in order to selectively deliver and/or controllably release one or more of said DNA alkylating agents. The agents, conjugates, and intermediates can be used to treat an illness that is characterized by undesired (cell) proliferation. As an example, the agents and the conjugates of this invention may be used to treat a tumor.