921928-01-0

Upstream product

• 771-61-9 2,3,4,5,6-pentafluorophenol 
• 7730-87-2 1-methylpiperidine-2-carboxylic acid 
• 41447-17-0 (R)-1-methylpiperidine-2-carboxylic acid 
• 1723-00-8 (R)-(+)-pipecolic acid 

Downstream Products

• 1017683-85-0 C₃₅H₅₁N₅O₆S 
• 936691-46-2 (2S,4R)-4-[[2-[(1R,3R)-1-acetoxy-4-methyl-3-[methyl-[(2S,3S)-3-methyl-2-[[(2R)-1-methylpiperidine-2-carbonyl]amino]pentanoyl]amino]pentyl]thiazole-4-carbonyl]amino]-2-methyl-5-phenyl-pentanoic acid 
• 1101181-40-1 C₄₂H₅₉N₅O₆S 
• 1101181-32-1 C₄₂H₅₉N₅O₆S 

Relevant academic research and scientific papers

CONJUGATION LINKERS CONTAINING 2,3-DIAMINOSUCCINYL GROUP

Provided is a conjugate of a cytotoxic drug/molecule to a cell-binding molecule with a bis-linker (adual-linker) containing a 2, 3-diaminosuccinyl group. It also relates to preparation of the conjugate of a cytotoxic drug/molecule to a cell-binding molecule with the bis-linker, particularly when the drug having functional groups of amino, hydroxyl, diamino, amino-hydroxyl, dihydroxyl, carboxyl, hydrazine, aldehyde and thiol for conjugation with the bis-linker in a specific manner, as well as the therapeutic use of the conjugates.

A CONJUGATE OF A TUBULYSIN ANALOG WITH BRANCHED LINKERS

The present invention relates to the conjugation of a tubulysin analog compound to a cell-binding molecule with branched/side-chain linkers for having better delivery of the conjugate compound and targeted treatment of abnormal cells. It also relates to a branched-linkage method of conjugation of a tubulysin analog molecule to a cell-binding ligand, as well as methods of using the conjugate in targeted treatment of cancer, infection and autoimmune disease.

TUBULYSINS AND PROTEIN-TUBULYSIN CONJUGATES

Provided herein are compounds, compositions, and methods for the treatment of diseases and disorders associated with cancer, including tubulysins and protein (e.g., antibody) drug conjugates thereof.

A CONJUGATE OF A TUBULYSIN ANALOG WITH BRANCHED LINKERS

The present invention relates to the conjugation of a tubulysin analog compound to a cell-binding molecule with branched/side-chain linkers for having better delivery of the conjugate compound and targeted treatment of abnormal cells. It also relates to a branched-linkage method of conjugation of a tubulysin analog molecule to a cell-binding ligand, as well as methods of using the conjugate in targeted treatment of cancer, infection and autoimmune disease.

CONJUGATION OF A CYTOTOXIC DRUG WITH BIS-LINKAGE

What provided is the conjugation of cytotoxic to a cell-binding molecule with a bis-linker(dual-linker) as shown in Formula (I). It provides bis-linkage methods of making a conjugate of a cytotoxic drug molecule to a cell-binding agent in a specific manner. It also relates to application of the conjugates for the treatment of a cancer, or an autoimmune disease, or an infectious disease.

CONJUGATION LINKERS, CELL BINDING MOLECULE-DRUG CONJUGATES CONTAINING THE LIKERS, METHODS OF MAKING AND USES SUCH CONJUGATES WITH THE LINKERS

The present invention relates to linkers having a group of propiolyl, substituted acryl (acryloyl), or disubstituted propanoyl, and using such linkers for the conjugation of compounds, in particular, cytotoxic agents to a cell-binding molecule.

TUBULYSIN CONJUGATE FOR USE IN TREATING CANCER

The invention described herein pertains to drug delivery conjugates for targeted therapy. The invention described herein relates to methods of treating folate receptor-expressing cancers with a folate-tubulysin conjugate. The invention described herein al

SPECIFIC CONJUGATION LINKERS, SPECIFIC IMMUNOCONJUGATES THEREOF, METHODS OF MAKING AND USES SUCH CONJUGATES THEREOF

The present invention relates to novel linkers containing a 2,3-disubstituted succinic group, or 2-monosubstituted, or 2,3-disubstituted fumaric or maleic (trans (E)- or cis (Z)- butenedioic), or acetylenedicarboxyl group for conjugation of a cytotoxic agent, and/or one or more different functional molecules per linker to a cell-binding molecule, through bridge linking pairs of thiols on the cell-binding molecule specifically. The invention also relates to methods of making such linkers, and of using such linkers in making homogeneous conjugates, as well as of application of the conjugates in treatment of cancers, infections and autoimmune disorders.

METHODS OF TREATING CANCER WITH TUBULYSIN CONJUGATES

The invention described herein pertains to drug delivery conjugates for targeted therapy. The invention described herein relates to methods of treating folate receptor-expressing cancers with a folate-tubulysin conjugate. The invention described herein al

CONJUGATES OF GARFTASE INHIBITORS

The invention described herein pertains to conjugates of GARFTase inhibitors. In particular, the invention described herein pertains to conjugates of GARFTase inhibitors that target the folate receptor for delivery of conjugated drugs to a mammalian recip