公开(公告)号：US20180280320A1

公开(公告)日：2018-10-04

申请号：US15934660

申请日：2018-03-23

Applicant: North Carolina Agricultural and Technical State University ,  North Carolina Central University

Inventor： Shengmin Sang ,  Yingdong Zhu ,  TinChung Leung

IPC: A61K31/12 ,  A61P1/18 ,  A61P9/00 ,  A61P25/02 ,  A61P27/02

CPC classification number: A61K31/12 ,  A61P1/18 ,  A61P9/00 ,  A61P25/02 ,  A61P27/02

Abstract: Derivatives of 6-shogaol are described herein. Also described herein are methods of preparing the derivatives, as well as methods of using the derivatives to activate Nrf2 and to treat diseases associated with inflammation and/or oxidative stress.

公开(公告)号：US20180162844A1

公开(公告)日：2018-06-14

申请号：US15880808

申请日：2018-01-26

Applicant: EA PHARMA CO., LTD.

Inventor： Kaori KOBAYASHI ,  Tamotsu Suzuki ,  Tatsuya Okuzumi

IPC: C07D405/14 ,  C07D405/12 ,  C07D491/048 ,  A61P11/06 ,  A61P17/04 ,  A61P1/18 ,  A61P1/04 ,  A61P19/02 ,  A61P25/02 ,  A61P37/08 ,  A61P29/00

CPC classification number: C07D405/14 ,  A61K31/443 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61P1/04 ,  A61P1/18 ,  A61P11/06 ,  A61P17/04 ,  A61P19/02 ,  A61P25/02 ,  A61P29/00 ,  A61P37/08 ,  C07D405/12 ,  C07D491/048

Abstract: Compounds represented by formula (I): wherein each symbol is as defined herein exhibit superior TRPA1 antagonist activity and are useful for the prophylaxis or treatment of diseases involving TRPA1 antagonist and TRPA1.

公开(公告)号：US20180148793A1

公开(公告)日：2018-05-31

申请号：US15575222

申请日：2016-05-19

Applicant: Fred Hutchinson Cancer Research Center

Inventor： Sunil R. HINGORANI

IPC: C12Q1/6886 ,  A61P35/00 ,  A61P1/18

CPC classification number: C12Q1/6886 ,  A61P1/18 ,  A61P35/00 ,  C12Q2600/118 ,  C12Q2600/156 ,  C12Q2600/158

Abstract: The instant disclosure provides methods for using biomarkers for identifying therapeutic regimens to treat pancreas cancer, or to reduce the risk of pancreas cancer, pancreas cancer metastasis, pancreas cancer proliferation, or pancreas cancer recurrence. For example, such therapeutic regimens can be based on the level of RUNX3 expression in the context of a particular DPC4 genotype, or based on the level of RUNX3 expression in combination with the level of Col6a1 expression, Spp1 expression or both. Such therapeutic regimens can include a main therapy, a neoadjuvant therapy, an adjuvant therapy, or any combination thereof. Also provided are methods for diagnosing or detecting metastatic potential of pancreas cancer cells based on the foregoing.

公开(公告)号：US20180098960A1

公开(公告)日：2018-04-12

申请号：US15567133

申请日：2016-04-18

Applicant: NADIANBIO

Inventor： Hong Seob SO ,  Hyung-Jin KIM ,  Aihua SHEN

IPC: A61K31/352 ,  A61K31/343 ,  A23L33/10

CPC classification number: A61K31/352 ,  A23L33/10 ,  A23V2002/00 ,  A23V2200/30 ,  A61K31/122 ,  A61K31/343 ,  A61P1/18

Abstract: The present invention relates to a composition for the prevention and treatment of pancreatitis comprising a naphthoquinone-based compound, a pharmaceutically acceptable salt, a prodrug, a solvate, or an isomer of the same. Particularly, the naphthoquinone-based compounds β-lapachone and dunnione can reduce the pancreatic weight/body weight ratio, which is increased by pancreatitis; reduce the increased activities of digestive enzymes (amylase and lipase); reduce the expressions of cytokines (IL-1β (interleukin-1β) and MCP-1); reduce or inhibit the inflammation, edema, and cell necrosis of the pancreatic tissues; and inhibit the lung damage caused by pancreatitis. Therefore, the naphthoquinone-based compound, the pharmaceutically acceptable salt, the pro-drug, the solvate, or the isomer thereof can be effectively used as a composition for the prevention and treatment of pancreatitis.

公开(公告)号：US12060367B2

公开(公告)日：2024-08-13

申请号：US18314445

申请日：2023-05-09

Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH ,  VANDERBILT UNIVERSITY

Inventor： Joachim Broeker ,  Jason Abbott ,  Jianwen Cui ,  Stephen W. Fesik ,  Julian Fuchs ,  Andreas Gollner ,  Lorenz Herdeis ,  Tim Hodges ,  Andrew Little ,  Andreas Mantoulidis ,  Jason Phan ,  Juergen Ramharter ,  Dhruba Sarkar ,  Christian Alan Paul Smethurst ,  Kevin Sokol ,  Heinz Stadtmueller ,  Qi Sun ,  Matthias Treu ,  Alex Waterson ,  Birgit Wilding ,  Tobias Wunberg

IPC: C07D498/10 ,  A61P1/00 ,  A61P1/18 ,  A61P11/00 ,  A61P17/00 ,  A61P35/00 ,  C07D519/00

CPC classification number: C07D498/10 ,  A61P1/00 ,  A61P1/18 ,  A61P11/00 ,  A61P17/00 ,  A61P35/00 ,  C07D519/00

Abstract: The present invention encompasses compounds of formula (I)






wherein R1a, R1b, R2a, R2b, Z, R3 to R5, A, p, U, V and W have the meanings given in the claims and specification, their use as inhibitors of KRAS, pharmaceutical compositions and preparations containing such compounds and their use as medicaments/medical uses, especially as agents for treatment and/or prevention of oncological diseases.

公开(公告)号：US20240261447A1

公开(公告)日：2024-08-08

申请号：US18293217

申请日：2022-07-25

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： James J. Moon ,  Cheng XU ,  Timothy FRANKEL ,  Peter SCOTT

IPC: A61K51/12 ,  A61K39/44 ,  A61K45/06 ,  A61K47/69 ,  A61K49/00 ,  A61K51/06 ,  A61P1/18

CPC classification number: A61K51/1244 ,  A61K39/44 ,  A61K45/06 ,  A61K47/6927 ,  A61K47/6929 ,  A61K47/6939 ,  A61K49/0091 ,  A61K49/0093 ,  A61K51/065 ,  A61P1/18

Abstract: The present invention relates to biodegradable agents associated with (e.g., complexed, conjugated, encapsulated, absorbed, adsorbed, admixed) one or more of a therapeutic agent (e.g., configured for treating, preventing or ameliorating various types of disorders), a diagnostic agent, and an agent capable of relaxing (e.g., opening, dilating) the hepatopancreatic anatomical region, as well as systems and methods utilizing such compositions (e.g., in diagnostic and/or therapeutic settings (e.g., treating pancreatic cancers)).

公开(公告)号：US20240226089A1

公开(公告)日：2024-07-11

申请号：US18095384

申请日：2023-01-10

Applicant: OCHSNER CLINIC FOUNDATION

Inventor： Richard N. RE, M.D. ,  Xin ZHANG, M.D., Ph.D. ,  Li LI, M.D., Ph.D.

IPC: A61K31/472 ,  A61K31/4178 ,  A61K31/4184 ,  A61K31/437 ,  A61P1/18 ,  A61P35/00

CPC classification number: A61K31/472 ,  A61K31/4178 ,  A61K31/4184 ,  A61K31/437 ,  A61P1/18 ,  A61P35/00

Abstract: Embodiments provide for methods of treatment for subjects suffering from a condition/disorder or disease for which the renin-angiotensin-aldosterone system (RAAS) plays at least some role. In one example, a method comprises administering to the subject an effective amount of one or more of an angiotensin receptor AT2R antagonist for a duration sufficient to elicit a desired response in the subject suffering from pancreatic cancer. The administering acts to reduce proliferation of tumor cells associated with the pancreatic cancer.

公开(公告)号：US12023306B2

公开(公告)日：2024-07-02

申请号：US17188023

申请日：2021-03-01

Applicant: SciCann Therapeutics Inc.

Inventor： Zohar Koren

IPC: A61K31/05 ,  A23L33/105 ,  A61K8/92 ,  A61K31/16 ,  A61K31/352 ,  A61K36/185 ,  A61K36/28 ,  A61K45/06 ,  A61P1/00 ,  A61P1/16 ,  A61P1/18 ,  A61P29/00 ,  A61P31/00 ,  A61Q19/00

CPC classification number: A61K31/05 ,  A23L33/105 ,  A61K8/922 ,  A61K31/16 ,  A61K31/352 ,  A61K36/185 ,  A61K36/28 ,  A61K45/06 ,  A61P1/00 ,  A61P1/16 ,  A61P1/18 ,  A61P29/00 ,  A61P31/00 ,  A61Q19/00 ,  A61K2800/92 ,  A61K36/28 ,  A61K2300/00 ,  A61K36/185 ,  A61K2300/00 ,  A61K31/16 ,  A61K2300/00 ,  A61K31/05 ,  A61K2300/00 ,  A61K31/352 ,  A61K2300/00

Abstract: Provided herein are fixed-dose combination (FDC) compositions comprising therapeutically effective amounts of at least one cannabinoid and spilanthol whether as essentially pure isolates or synthetics or as components of essential oils or plant extracts or combinations thereof. The compositions are formulated as pharmaceutical compositions, nutraceuticals, cosmeceuticals, nutricosmetics, cosmetics, or food products. The pharmaceutical compositions are useful for the treatment of a gastro-enteric disease selected from the group consisting of irritable bowel disease, Crohn's disease, colitis, irritable bowel syndrome, and acute and chronic pancreatitis or of sepsis. Other pharmaceutical uses are as anti-allergic, anti-inflammatory, immunomodulator, antioxidant, anti-microbial, antibacterial, antifungal, antiviral, antinociceptive, analgesic, anesthetic, anti-cancer, apoptosis inducing, antiscorbutic, antipyretic, anti-malarial, addiction mitigatory, anxiolytic, anti-depressant, diuretic, anti-diarrheal, vasodilator or aphrodisiac agents. The pharmaceutical compositions of this invention exhibit a synergistic effect.

公开(公告)号：US20240174690A1

公开(公告)日：2024-05-30

申请号：US18314445

申请日：2023-05-09

Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH ,  VANDERBILT UNIVERSITY

Inventor： Joachim BROEKER ,  Jason ABBOTT ,  Jianwen CUI ,  Stephen W. FESIK ,  Julian FUCHS ,  Andreas GOLLNER ,  Lorenz HERDEIS ,  Tim HODGES ,  Andrew LITTLE ,  Andreas MANTOULIDIS ,  Jason PHAN ,  Juergen RAMHARTER ,  Dhruba SARKAR ,  Christian Alan Paul SMETHURST ,  Kevin SOKOL ,  Heinz STADTMUELLER ,  Qi SUN ,  Matthias TREU ,  Alex WATERSON ,  Birgit WILDING ,  Tobias WUNBERG

IPC: C07D498/10 ,  A61P1/00 ,  A61P1/18 ,  A61P11/00 ,  A61P17/00 ,  A61P35/00 ,  C07D519/00

CPC classification number: C07D498/10 ,  A61P1/00 ,  A61P1/18 ,  A61P11/00 ,  A61P17/00 ,  A61P35/00 ,  C07D519/00

Abstract: The present invention encompasses compounds of formula (I)




wherein R1a, R1b, R2a, R2b, Z, R3 to R5, A, p, U, V and W have the meanings given in the claims and specification, their use as inhibitors of KRAS, pharmaceutical compositions and preparations containing such compounds and their use as medicaments/medical uses, especially as agents for treatment and/or prevention of oncological diseases.

公开(公告)号：US20240150423A1

公开(公告)日：2024-05-09

申请号：US17768236

申请日：2020-11-09

Applicant: Nanjing Finepeptide Biopharmaceutical Co.,Ltd

Inventor： Song-Shan Tang ,  Qun Luo ,  Xu-Dong Zhang ,  Jing-Xuan TANG ,  Li Yang ,  Hong-Mei Tan

IPC: C07K14/605 ,  A61P1/18 ,  A61P3/10

CPC classification number: C07K14/605 ,  A61P1/18 ,  A61P3/10 ,  A61K38/00

Abstract: Applications of different configurations of novel glucagon peptide 1 with fatty acid modification or nonmodification in the treatment of T2D or the pancreas protection are provided. The dimer of the present disclosure is formed by two identical cysteine-containing GLP-1 monomers through a disulfide bond. The H-like GLP-1 homodimer (disulfide bond is inside chains) showed remarkable increase in hypoglycemic duration without reducing specific activity. The GLP-1 dimer provided has an in-vivo effective duration of up to 19 days, which significantly prolonged compared with that of the positive control drug Liraglutide with 3 days of effective duration, or thereby greatly promoting the technical advancement in long-acting GLP-1 drugs and facilitating their clinical applications and business. Meanwhile the U-like homodimer (disulfide bond is at the C-terminus) does not affect blood glucose, but can obviously protect pancreatic exocrine cells such as acini and ducts, and improve pancreas function.