公开(公告)号：US20180148487A1

公开(公告)日：2018-05-31

申请号：US15578094

申请日：2015-07-31

Applicant: AJOU UNIVERSITY INDUSTRY-ACADEMIC COOPERATION FOUNDATION

Inventor： Sang Dun CHOI ,  Tae Hyeon YOO ,  Seol Hee PARK

IPC: C07K14/47 ,  C07K7/08 ,  A61P29/00 ,  C07K16/28

CPC classification number: C07K14/4703 ,  A61K38/00 ,  A61P29/00 ,  A61P37/00 ,  C07K7/08 ,  C07K14/47 ,  C07K16/2896

Abstract: The present disclosure relates to a peptide for inhibiting a TLR4 signaling pathway, a TLR4 antagonist including the peptide, and a composition for preventing or treating autoimmune diseases and inflammatory diseases. More specifically, the present disclosure relates to a peptide which binds to a TLR4/MD2 composite to inhibit the secretion of interleukin-6 (IL-6), NO, and ROS, and the activation of NFκB and MAPKs, a TLR4 antagonist including the peptide, and a composition for preventing or treating autoimmune diseases and inflammatory diseases. The peptide according to the present disclosure has an excellent effect of inhibiting the secretion of interleukin-6 (IL-6), NO, and ROS, and the activation of NFκB and MAPKs by inhibiting a TLR4 signaling pathway induced by a liphopolysaccharide (LPS), and thus can be favorably used as a composition for preventing or treating autoimmune diseases and inflammatory diseases occurring by the TLR4 signaling pathway.

公开(公告)号：US20230000861A1

公开(公告)日：2023-01-05

申请号：US17774346

申请日：2020-11-05

Applicant: AJOU UNIVERSITY INDUSTRY-ACADEMIC COOPERATION FOUNDATION ,  UNIVERSITY-INDUSTRY COOPERATION GROUP OF KYUNG HEE UNIVERSITY

Inventor： Sang Dun CHOI ,  Mahesh Chandra PATRA ,  Nasir JAVAID ,  Maria BATOOL ,  Dae-Hyun HAHM

IPC: A61K31/502 ,  A61P29/00 ,  A61P37/00 ,  C07D417/14 ,  C07D417/12

Abstract: A small molecule TNF-α inhibitor is disclosed. The compound has an activity of inhibiting the formation of a TNF-α homotrimer by specifically binding to the binding cavity of a TNF-α homodimer. A composition containing the compound as well as uses of the compound and the composition in preventing or treating autoimmune diseases and/or inflammatory diseases are disclosed. Extracellular inactivation of TNF-α through protein-protein interface destruction is the most innovative and effective method for alleviating chronic systemic inflammatory states, and TIM series compounds, which have better efficacy and lower toxicity than those of existing TNF inhibitors and have oral bioavailability, can be effectively used as leading anti-inflammatory molecules.

公开(公告)号：US20200299330A1

公开(公告)日：2020-09-24

申请号：US16858071

申请日：2020-04-24

Applicant: AJOU UNIVERSITY INDUSTRY-ACADEMIC COOPERATION FOUNDATION

Inventor： Moon Suk KIM ,  Sang Dun CHOI ,  Seung Hun PARK ,  Masaud SHAH

IPC: C07K7/06 ,  A61P17/02

Abstract: A substance P analog having a progenitor cell or stem cell recruiting activity and a method of recruiting progenitor cells or stem cells using the substance P analog are disclosed. The substance P analog has an effect of recruiting endogenous progenitor cells or stem cells to a wound or disease-occurring site. Thus, the disclosure also describes its use in recruiting progenitor cells or stem cells and a method of regenerating or treating a damaged organ or tissue, or a method of healing a wound.

公开(公告)号：US20180148455A1

公开(公告)日：2018-05-31

申请号：US15578086

申请日：2015-12-23

Applicant: AJOU UNIVERSITY INDUSTRY-ACADEMIC COOPERATION FOUNDATION

Inventor： Sang Dun CHOI ,  Prasannavenkatesh DURAI ,  Asma ACHEK

IPC: C07D487/04 ,  C07D409/12 ,  C07D211/26 ,  C07D243/08 ,  C07C251/24 ,  C07D265/30 ,  C07D401/12 ,  C07D471/10 ,  C07D211/34 ,  C07D401/14 ,  C07D403/06 ,  C07D403/12 ,  C07D401/06 ,  C07D333/78 ,  C07D207/277 ,  C07D471/04 ,  A61P7/00 ,  A61P17/00 ,  A61P37/08 ,  A61P11/06 ,  A61P27/02 ,  A61P1/02 ,  A61P27/00 ,  A61P27/16 ,  A61P1/00 ,  A61P31/12 ,  A61P11/00 ,  A61P1/04 ,  A61P19/06 ,  A61P19/02 ,  A61P29/00 ,  A61P13/12 ,  A61P25/28

CPC classification number: C07D487/04 ,  A61K9/0053 ,  A61K31/4178 ,  A61K31/4453 ,  A61K31/496 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/551 ,  A61P1/00 ,  A61P1/02 ,  A61P1/04 ,  A61P7/00 ,  A61P11/00 ,  A61P11/06 ,  A61P13/12 ,  A61P17/00 ,  A61P19/02 ,  A61P19/06 ,  A61P25/28 ,  A61P27/00 ,  A61P27/02 ,  A61P27/16 ,  A61P29/00 ,  A61P31/12 ,  A61P37/08 ,  C07C251/24 ,  C07D207/277 ,  C07D211/26 ,  C07D211/34 ,  C07D243/08 ,  C07D265/30 ,  C07D333/78 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/06 ,  C07D403/12 ,  C07D409/12 ,  C07D471/04 ,  C07D471/10

Abstract: The present disclosure relates to a novel small molecule TLR2 antagonist, and particularly, to 19 novel TLR2 antagonists, a pharmaceutical composition, including the antagonists, for preventing or treating inflammatory diseases, and a TLR4 regulator.The novel TLR2 antagonists according to the present disclosure can be effectively used as a preparation for oral administration by having low molecular weight and high oral bioavailability, and can be useful in pharmaceutical compositions for preventing or treating inflammatory diseases since the secretion of IL-8 is effectively inhibited and in vivo cytotoxicity is not induced. In addition, the novel TLR2 antagonists according to the present disclosure can be used as a TLR4 regulator.