C07K5/06052

Synthesis and intermediates of pyrrolobenzodiazepine derivatives for conjugation
09745303 · 2017-08-29 · ·

A method of synthesing a compound of formula (I) from a compound of formula (III). ##STR00001##

PYRROLOBENZODIAZEPINES AND CONJUGATES THEREOF

A conjugate comprising a PBD dimer linked from the tether joining the two PBD units, wherein the linker is of formula (A1): (Formula (A1)) wherein R.sup.N1 is selected from H and C.sub.1-4 alkyl; L is a linker connected to a cell binding agent; CBA is the cell binding agent; n is an integer selected in the range of 0 to 48; Q is: (Formula (Q)), where Q.sup.x is such that Q is an amino-acid residue, a dipeptide residue or a tripeptide residue.

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COMPOSITIONS AND METHODS FOR TREATING COLORECTAL CANCER
20170224759 · 2017-08-10 ·

The present invention relates to methods of treating a patient who has colorectal cancer and to methods of reducing the likelihood that a patient will develop or experience a recurrence of colorectal cancer. The methods comprise a step of introducing, to the patient, an effective amount of an agent that targets an intestinal H.sup.−-coupled di/tripeptide transporter (PepT1). Useful compositions including, for example, the tripeptide KPV, vectors encoding such peptides, and cells (e.g., bacterial cells) including them, are also within the scope of the present invention, as are kits including such compositions.

NOVEL LINKERS
20220031858 · 2022-02-03 ·

The invention relates to novel linkers which comprise two or three basic, acidic or hydrophobic natural or non-natural amino acids. The invention also relates to drug conjugates comprising said linkers, to pharmaceutical compositions comprising said drug conjugates and to the use of said drug conjugates in preventing, suppressing or treating cancer.

PEPTIDE ACETALS FOR STABILISING ENZYMES
20220267699 · 2022-08-25 ·

The present invention relates to a compound for stabilizing enzymes, the use of said compound for stabilizing an enzyme, a composition comprising said compound, a method of preparing the composition comprising said compound, a detergent composition comprising said compound and a method of preparing said compound.

Proteasome inhibitors

The disclosure provides proteasome inhibitors that can be used to halt cell division of rapidly dividing cells by preventing the degradation of cell cycle-regulating proteins, such as cyclins, cyclin-dependent kinase inhibitors, and p53. The proteasome inhibitor compounds can be used to inhibit the proliferation of cancer cells.

Metal compound having phase transformation and method of preparing the same
11396453 · 2022-07-26 · ·

The present invention relates to a metal phase transformation compound and a method for preparing the same.

METHODS, COMPOUNDS, COMPOSITIONS AND VEHICLES FOR DELIVERING 3-AMINO-1-PROPANESULFONIC ACID

The invention relates to methods, compounds, compositions and vehicles for delivering 3-amino-1-propanesulfonic acid (3APS) in a subject, preferably a human subject. The invention encompasses compound that will yield or generate 3APS, either in vitro or in vivo. Preferred compounds include amino acid prodrugs of 3APS for use, including but not limited to the prevention and treatment of Alzheimer's disease

PYRROLOBENZODIAZEPINE CONJUGATES
20210380605 · 2021-12-09 ·

A compound of formula (I) and salts and solvates thereof, wherein R.sup.L is a linker for connection to a cell binding agent, which is formula (IIa) wherein Q is a tripeptide residue of formula (A), where x is 1 or 2, —C(═O)-Q.sup.x-NH— is a dipeptide residue; X is: formula (B), where a=0 to 5, b=0 to 16, c=0 or 1, d=0 to 5; and G.sup.L is a linker for connecting to a Ligand Unit.

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AMIDE DERIVATIVES OF N-UREA SUBSTITUTED AMINO ACIDS AS FORMYL PEPTIDE RECEPTOR LIKE-1 (FPRL-1) RECEPTOR MODULATORS

The present invention relates to novel amide derivatives of N-urea substituted amino acids, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.