Legochem Biosciences, Inc.

Ligachem Biosciences Inc.

Jeong Hee Ryu

Yong Zu Kim

Jeiwook Chae

Chul-Woong Chung

Yeong Soo Oh

Ho Young Song

Yun Hee Park

Sun Young Kim

Sung Ho Woo

Hyang Sook Lee

Tae Kyo Park

Kyu Man Oh

Ji Young Min

Jong Un Cho

Doo Hwan Jung

Jeon Yang

Sang Eun Chae

Dae Yon Lee

Hyun Jin Kwon

Yoon Jeong Choi

Eun Mi Jung

Eun Hye Yang

Eun Hye Ban

Yun Ki Kim

Ju Hyun Shin

Ji Eun Jung

Hyo Jung Choi

The present invention relates to novel compounds as autotoxin inhibitors for treatment and prophylaxis of conditions or a disorder caused by autotaxin activation or increased concentration of lysophosphatidic acid, and also a pharmaceutical composition containing the same. The novel compounds of the present invention are autotoxin inhibitors, and by inhibiting the production of lysophosphatidic acid, they are useful for treatment or prophylaxis of cardiovascular disorder, cancer, metabolic disorder, kidney disorder, liver disorder, inflammatory disorder, nervous system disorder, respiratory system disorder, fibrotic disease, ocular disorder, cholestatic and other forms of chronic pruritus, or acute or chronic organ transplant rejection.

Compounds as autotaxin inhibitors and pharmaceutical compositions comprising the same

Provided herein are compounds comprising a self-immolative group, and the compounds comprising a self-immolative group according to the present invention may include a protein (for example, an oligopeptide, a polypeptide, an antibody, or the like) having substrate-specificity for a target and an active agent (for example, a drug, a toxin, a ligand, a detection probe, or the like) having a specific function or activity.

Compounds comprising self-immolative group

Provided are compounds comprising a self-immolative group, and the compounds comprising a self-immolative group according to the present invention may include a protein (for example, an oligopeptide, a polypeptide, an antibody, or the like) having substrate-specificity for a target and an active agent (for example, a drug, a toxin, a ligand, a detection probe, or the like) having a specific function or activity.

In some aspects, the invention relates to an antibody-drug conjugate, comprising an anti-CD19 antibody; a linker; and an active agent. The antibody-drug conjugate may comprise a self-immolative group. The linker may comprise an O-substituted oxime, e.g., wherein the oxygen atom of the oxime is substituted with a group that covalently links the oxime to the active agent; and the carbon atom of the oxime is substituted with a group that covalently links the oxime to the antibody.

Compositions and methods related to anti-CD19 antibody drug conjugates

In some aspects, the invention relates to an antibody-drug conjugate, comprising an anti-epidermal growth factor receptor ('EGFR') antibody; a linker; and an active agent. The antibody-drug conjugate may comprise a self-immolative group. The linker may comprise an O-substituted oxime, e.g., wherein the oxygen atom of the oxime is substituted with a group that covalently links the oxime to the drug; and the carbon atom of the oxime is substituted with a group that covalently links the oxime to the antibody.

Compositions and methods related to anti-EGFR antibody drug conjugates

Provided are methods of use of compounds comprising a self-immolative group, which compounds may include a protein (for example, an oligopeptide, a polypeptide, an antibody, or the like) having substrate-specificity for a target and an active agent (for example, a drug, a toxin, a ligand, a detection probe, or the like) having a specific function or activity.

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Daejeon, South Korea

Jeong Hee Ryu