公开(公告)号：US11479528B2

公开(公告)日：2022-10-25

申请号：US16496355

申请日：2018-03-20

Applicant: TAIPEI MEDICAL UNIVERSITY

Inventor： Jing-ping Liou ,  Che-ming Teng ,  Shiow-lin Pan

IPC: C07C235/60 ,  C07C49/835 ,  A61K9/00 ,  C07D295/135 ,  C07D295/192 ,  C07D213/75 ,  C07D209/08 ,  C07D471/04 ,  C07D231/56 ,  C07D487/04 ,  C07D215/38 ,  C07D261/20 ,  C07C233/75 ,  C07C311/21 ,  C07C39/15 ,  A61P35/00

Abstract: This disclosure is related to aromatic compounds of formula (I), and methods of their use in treating medical conditions associated with Heat Shock Protein-90 (HSP90), e.g., cancer. Compounds of formula (I) have the following structure: Also disclosed are pharmaceutical compositions comprising compounds of formula (I).

公开(公告)号：US20220194929A1

公开(公告)日：2022-06-23

申请号：US17470464

申请日：2021-09-09

Applicant: CHEMOCENTRYX, INC.

Inventor： Trevor T. CHARVAT ,  Junfa FAN ,  Christopher W. LANGE ,  Manmohan Reddy LELETI ,  Yandong LI ,  Venkat Reddy MALI ,  Jeffrey P. McMAHON ,  Jay POWERS ,  Sreenivas PUNNA ,  Ju YANG

IPC: C07D413/06 ,  C07D401/04 ,  C07D403/06 ,  C07D405/06 ,  C07D417/04 ,  C07D211/56 ,  C07D295/135 ,  C07D211/62 ,  C07D401/06 ,  C07D211/26 ,  C07D211/70 ,  C07D241/04 ,  C07D207/16 ,  C07D211/34 ,  A61K31/451 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/495 ,  A61K31/496 ,  A61K31/5377

Abstract: Aniline compounds are provided which bind to CCR(4) and are useful for the treatment of diseases such as allergic diseases, autoimmune diseases, graft rejection and cancer.

公开(公告)号：US11274077B2

公开(公告)日：2022-03-15

申请号：US16909712

申请日：2020-06-23

Applicant: Eastern Virginia Medical School ,  The Regents of the Univ. of California Santa Cruz ,  The U.S. Dept of Health & Human Services ,  Thomas Jefferson University

Inventor： David J. Maloney ,  Diane K. Luci ,  Ajit Jadhav ,  Theodore Holman ,  Jerry L. Nadler ,  Michael Holinstat ,  David Taylor-Fishwick ,  Anton Simeonov ,  Adam Yasgar ,  Steven McKenzie

IPC: C07C311/44 ,  A61P7/02 ,  C07D211/28 ,  C07D213/76 ,  C07D217/02 ,  C07D217/22 ,  C07D235/30 ,  C07D239/69 ,  C07D261/16 ,  C07D263/58 ,  C07D277/52 ,  C07D277/82 ,  C07D295/135 ,  C07D333/36 ,  C07D417/12

Abstract: Human lipoxygenases (LOXs) are a family of iron-containing enzymes involved in catalyzing the oxidation of polyunsaturated fatty acids to provide the corresponding bioactive hydroxyeicosatetraenoic acid (HETE) metabolites. These eicosanoid signaling molecules are involved in a number of physiologic responses such as platelet aggregation, inflammation, and cell proliferation. Platelet-type 12-(S)-LOX (12-LOX) is of particular interest because of its demonstrated role in skin diseases, diabetes, platelet hemostasis, thrombosis, and cancer. Disclosed herein is the identification and medicinal chemistry optimization of a 4-((2-hydroxy-3-methoxybenzyl)amino)benzenesulfonamide-based scaffold. The compounds display nM potency against 12-LOX and excellent selectivity over related lipoxygenases and cyclooxygenases. In addition to possessing favorable ADME properties, the compounds also inhibit PAR-4 induced aggregation and calcium mobilization in human platelets, and reduce 12-HETE in mouse/human beta cells. The compounds can also be used in methods for treating or preventing a 12-lipoxygenase mediated disease or disorder.

公开(公告)号：US11118065B2

公开(公告)日：2021-09-14

申请号：US16485724

申请日：2018-02-11

Applicant: CHANGZHOU TRONLY ADVANCED ELECTRONIC MATERIALS CO., LTD. ,  CHANGZHOU TRONLY NEW ELECTRONIC MATERIALS CO., LTD.

Inventor： Xiaochun Qian

IPC: C08F2/46 ,  C08F2/50 ,  C08G61/04 ,  C09D4/00 ,  C07C45/41 ,  C07C45/63 ,  C07C221/00 ,  C07C225/18 ,  C07D265/30 ,  C07D295/135 ,  C09D11/037 ,  C09D11/101 ,  C09D11/107 ,  G03F7/029 ,  C08K5/17 ,  C08K5/3435 ,  C08K5/357

Abstract: A fluorenylaminoketone photoinitiator, a preparation method thereof, and a UV photocurable composition containing same. The photoinitiator has a compound having a structure as shown in general formula (I) or a derivative compound thereof. The fluorenylaminoketone photoinitiator may effectively improve the solubility of traditional photoinitiators and reduce the use of micromolecular active diluents, and may also have high sensitivity and good deep-layer curing. It has very good promotion effect on popularization and application of photocurable compositions, particularly colored ink systems, in the field of photocuring. A UV photocurable composition containing such a fluorenylaminoketone photoinitiator can have an advantage in terms of high sensitivity, no residue after development, good pattern integrity, no or little odor of coating layers after curing, or excellent yellowing resistance.

公开(公告)号：US11084786B2

公开(公告)日：2021-08-10

申请号：US16907084

申请日：2020-06-19

Applicant: CALGENT BIOTECHNOLOGY CO., LTD.

Inventor： Yun Yen ,  Jing-Ping Liou ,  Shiow-Lin Pan

IPC: A61K31/40 ,  A61K31/166 ,  A61K31/122 ,  C07D207/04 ,  A61K45/06 ,  A61P35/00 ,  C07D295/135 ,  C07D295/13 ,  C07C311/29 ,  C07C237/34 ,  C07D213/40 ,  C07C225/30 ,  C07C255/58 ,  C07D209/08 ,  C07D209/44 ,  C07D215/38 ,  C07D215/40 ,  A61K31/7048 ,  C07C235/54 ,  A61K33/243 ,  A61P25/14 ,  A61P25/28 ,  A61P3/10 ,  C07C237/48

Abstract: The invention relates to new compounds with low cytotoxicity for blocking ubiquitination-proteasome system in diseases. Accordingly, these compounds can be used in treatment of treating disorders including, but not limited to, cancers, neurodegenerative diseases, inflammatory disorders and autoimmune disorders and metabolic disorders.

公开(公告)号：US20210122750A1

公开(公告)日：2021-04-29

申请号：US17080247

申请日：2020-10-26

Applicant: Saint Louis University

Inventor： Daniela Salvemini ,  Christopher K. Arnatt

IPC: C07D471/04 ,  C07D217/06 ,  C07D295/135 ,  A61P23/00 ,  A61P25/02

Abstract: Disclosed herein are compositions and methods for treating neuropathic pain in a subject in need thereof. Compositions disclosed herein are GPR183 antagonists. The methods include administering to a subject in need thereof a therapeutically effective amount of a GPR183 antagonist.

公开(公告)号：US20210115008A1

公开(公告)日：2021-04-22

申请号：US16970169

申请日：2019-02-15

Applicant: Constellation Pharmaceuticals, Inc.

Inventor： Jonathan E. Wilson ,  Francois Brucelle ,  Julian R. Levell

IPC: C07D401/04 ,  C07D231/12 ,  C07D237/08 ,  C07D295/135 ,  C07D401/14 ,  C07D403/04 ,  C07D405/04 ,  C07D213/75 ,  C07D231/40 ,  C07D487/04 ,  C07D491/107 ,  C07D413/04 ,  C07D417/04 ,  C07D209/08 ,  C07D215/08

Abstract: Provided are compounds of Formula (I): and pharmaceutically acceptable salts and compositions thereof, which are useful for treating a variety of conditions associated with histone acetyltransferase (HAT).

公开(公告)号：US20210087163A1

公开(公告)日：2021-03-25

申请号：US17108668

申请日：2020-12-01

Applicant: NORTH CAROLINA CENTRAL UNIVERSITY ,  THE UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL

Inventor： ALFRED L. WILLIAMS ,  JOHN E. SCOTT ,  LI-AN YEH ,  MATTHEW R. REDINBO

IPC: C07D333/34 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  A61K31/137 ,  A61K31/42 ,  A61K31/4409 ,  A61K31/4709 ,  A61K31/553 ,  C07D295/135 ,  C07D409/06 ,  C12Q1/34

Abstract: This invention relates generally to compounds that are glucuronidase inhibitors. The glucuronidase inhibitors include phenoxy thiophene sulfonamides, and other compounds such as pyridine sulfonyls, benzene sulfonyls, thiophene sulfonyls, thiazole sulfonyls, thiophene carbonyls, and thiazole carbonyls. These compounds include nialamide, isocarboxazid, phenelzine, amoxapine, loxapine and mefloquine. Also compositions including one or more of such compounds for use in inhibiting glucuronidase and methods of using one or more of such compounds for selective inhibition of bacterial β-glucoronidase. These compounds may be used as a co-drug in combination with the anticancer drug CPT-11. Also a method for screening compounds to determine their usefulness in reducing diarrhea associated with irinotecan chemotherapy.

公开(公告)号：US10899702B2

公开(公告)日：2021-01-26

申请号：US15546833

申请日：2016-02-05

Applicant: UNIVERSITY OF PITTSBURGH—OF THE COMMONWEALTH SYSTEM OF HIGHER EDUCATION

Inventor： Xiang-Qun Xie ,  Zhiwei Feng

IPC: C07C275/30 ,  C07C275/34 ,  C07C275/40 ,  C07C275/42 ,  C07D295/135 ,  C07C275/32

Abstract: Novel diphenylurea and benzylbenzenesulfonamide compounds are disclosed along with methods of inhibiting the activity of TRPV1 and methods of treating pain associated with transient receptor potential vanilloid type 1 (TRPV1) using such compounds.

公开(公告)号：US20210009552A1

公开(公告)日：2021-01-14

申请号：US17038690

申请日：2020-09-30

Applicant: Neoculi Pty Ltd.

Inventor： Stephen Page ,  Andrew Stevens ,  Adam McCluskey ,  Martine Keenan ,  Rebecca Abraham

IPC: C07D333/58 ,  A61K31/155 ,  A61K31/381 ,  C07C281/18 ,  C07D239/50 ,  C07D295/135 ,  A61K31/17 ,  A61K31/341 ,  A61K31/4045 ,  A61K31/4192 ,  A61K31/44 ,  A61K31/498 ,  C07C47/565 ,  C07C211/29 ,  C07C251/24 ,  C07D209/14 ,  C07D239/48 ,  C07D241/20 ,  C07D249/14 ,  C07D251/54 ,  C07D307/56 ,  C07D311/58 ,  C07D401/14 ,  A61K9/00 ,  A61K31/404 ,  A61K31/496 ,  A61K31/505 ,  A61K45/06 ,  C07C335/40 ,  C07D209/08

Abstract: The invention provides compounds of Formula (I), and their use in methods for treating or preventing a protozoan infection in a subject using a compound of Formula (I). The invention also provides the use of a compound of Formula (I) in the manufacture of a medicament for the treatment of a protozoan infection in a subject. The invention further provides a medical device when used in a method of treating or preventing a protozoan infection in a subject and to a medical device comprising the composition of the invention.