公开(公告)号：US20240279191A1

公开(公告)日：2024-08-22

申请号：US18694815

申请日：2022-09-22

申请人： The General Hospital Corporation

发明人： Xu Wu ,  Lu Hu

IPC分类号： C07D295/192 ,  A61P35/00 ,  C07D211/22 ,  C07D213/30 ,  C07D213/75 ,  C07D239/42 ,  C07D249/06 ,  C07D295/26 ,  C07D305/08 ,  C07D309/06

CPC分类号： C07D295/192 ,  A61P35/00 ,  C07D211/22 ,  C07D213/30 ,  C07D213/75 ,  C07D239/42 ,  C07D249/06 ,  C07D295/26 ,  C07D305/08 ,  C07D309/06

摘要： The present disclosure relates to compounds of Formula (I), and pharmaceutically acceptable salts thereof, compositions comprising same, and methods of using the compounds and compositions to treat various cancers.

公开(公告)号：US11883386B2

公开(公告)日：2024-01-30

申请号：US17815391

申请日：2022-07-27

申请人： Akebia Therapeutics, Inc.

发明人： Richard Masaru Kawamoto ,  Shengde Wu ,  Artem G. Evdokimov ,  Kenneth D Greis ,  Angelique Sun Boyer ,  Namal C. Warshakoon

IPC分类号： C07D213/81 ,  C07D213/65 ,  A61K31/4418 ,  C07C235/60 ,  C07C237/42 ,  C07C255/57 ,  C07D405/10 ,  C07D405/04 ,  C07D295/192 ,  C07D401/04 ,  C07D401/10 ,  C07D417/04 ,  A61K31/4433

CPC分类号： A61K31/4418 ,  A61K31/4433 ,  C07C235/60 ,  C07C237/42 ,  C07C255/57 ,  C07D213/65 ,  C07D213/81 ,  C07D295/192 ,  C07D401/04 ,  C07D401/10 ,  C07D405/04 ,  C07D405/10 ,  C07D417/04 ,  Y02A50/30

摘要： The present disclosure relates to HIF-1α prolyl hydroxylase inhibitors, compositions which comprise the HIF-1α prolyl hydroxylase inhibitors described herein and to methods for controlling, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia.

公开(公告)号：US11873380B2

公开(公告)日：2024-01-16

申请号：US17053431

申请日：2019-05-07

申请人： Tokyo University of Science Foundation

发明人： Koji Arimitsu

IPC分类号： C08K5/34 ,  C08K5/3435 ,  C07D295/192 ,  C07D307/88 ,  C08F20/32

CPC分类号： C08K5/3435 ,  C07D295/192 ,  C07D307/88 ,  C08F20/32

摘要： A photoreactive composition including a base-reactive compound, a photobase generator that is represented by the following Formula (1) and that generates a base when irradiated with light, and at least one compound selected from the group consisting of a polycyclic aromatic compound having a fused ring structure having two or more rings and a polycyclic aromatic compound having three or more aromatic rings and having a conjugated structure including any two or more of the three or more aromatic rings, in which the base-reactive compound is a compound having two or more groups that will have their polarity converted by the action of a base and that exhibit reactivity, in one molecule, or a compound having two or more groups that will react under the action of a base, in one molecule.

公开(公告)号：US20220411389A1

公开(公告)日：2022-12-29

申请号：US17713949

申请日：2022-04-05

申请人： Mayo Foundation for Medical Education and Research

发明人： John A. Copland, III ,  Han W. Tun ,  Thomas R. Caulfield ,  Christina Von Roemeling ,  Laura Ann Marlow

IPC分类号： C07D295/192 ,  A61K45/06 ,  C07D213/75 ,  C07D211/64 ,  C07D213/64 ,  A61K31/496 ,  A61K31/44 ,  A61K31/495 ,  C07D211/66

摘要： This document provides compounds, compositions, and methods for treating cancers including renal cancer (e.g., renal cell carcinoma) as well as ovarian, breast, prostate, colon, pancreatic, bladder, liver, lung, and thyroid cancers and melanoma. For example, compounds, compositions, and methods for using one or more inhibitors of SCD1 to treat renal cell carcinoma (e.g., clear cell renal cell carcinoma (ccRCC)), thyroid cancer, or liver cancer; or to increase the efficacy of treatment for the same.

公开(公告)号：US11414375B2

公开(公告)日：2022-08-16

申请号：US16894435

申请日：2020-06-05

申请人： Jiangxi Normal University

发明人： Junfeng Zhao ,  Long Hu ,  Silin Xu ,  Zhenguang Zhao

IPC分类号： C07C219/20 ,  C07C303/40 ,  C07D231/56 ,  C07D333/68 ,  C07C311/17 ,  C07C231/02 ,  C07C233/05 ,  C07D263/22 ,  C07D209/20 ,  C07D307/68 ,  C07C269/06 ,  C07C239/22 ,  C07D209/14 ,  C07D295/13 ,  C07K5/078 ,  C07D295/192 ,  C07D493/10 ,  C07K5/062 ,  C07K5/072 ,  C07D495/04 ,  C07C213/08

摘要： Disclosed are a mild and efficient preparation method for an α-acyloxyenamide compound and a use thereof in the synthesis of an amide and a polypeptide. The α-acyloxyenamide compound is obtained by an addition reaction of a ynamide and a carboxylic acid in dichloromethane under conditions where the temperature is 0° C. to 50° C.; the produced α-acyloxyenamide compound can react with an amine compound to produce an amide or a polypeptide; the two reactions can be carried out step by step, and can also be carried out in one pot. According to the invention, the reaction conditions are mild and no metal catalyst is required; when the carboxylic acid, which has chirality on an alpha site of carboxyl, forms an amide bond or a peptide bond, no racemization occurs; and the operation is simple and the application range is wide.

公开(公告)号：US20220213030A1

公开(公告)日：2022-07-07

申请号：US17599694

申请日：2020-04-01

申请人： OSPEDALE SAN RAFFAELE SRL

发明人： Gianvito MARTINO ,  Luca MUZIO ,  Nilo RIVA ,  Davide GORNATI ,  Pierfausto SENECI ,  Simona Carmen ELEUTERI

IPC分类号： C07C281/18 ,  A61P25/28 ,  C07C277/08 ,  C07D295/192 ,  C07C311/08 ,  C07C311/21 ,  C07D233/88

摘要： The present invention relates to novel aminoguanidine hydrazone-derivatives of Formula (I) which are effective as retromer stabilizers and useful as neuroprotecting drugs. The invention also relates to pharmaceutical compositions comprising the compounds and their use in therapy and diagnostic.

公开(公告)号：US20220204497A1

公开(公告)日：2022-06-30

申请号：US17599931

申请日：2020-03-30

申请人： MEDICINAL BIOCONVERGENCE RESEARCH CENTER ,  DONGGUK UNIVERSITY INDUSTRY-ACADEMIC COOPERATION FOUNDATION

发明人： Sunghoon KIM ,  Dae Gyu KIM ,  Kyeong LEE ,  Minkyoung KIM

IPC分类号： C07D417/12 ,  A61P35/02 ,  C07D413/14 ,  C07D413/12 ,  C07D413/04 ,  C07D409/12 ,  C07D401/04 ,  C07D401/12 ,  C07D403/06 ,  C07D405/12 ,  C07D333/34 ,  C07D295/13 ,  C07D295/135 ,  C07D295/192 ,  C07D317/68 ,  C07D285/135 ,  C07D277/46 ,  C07D277/40 ,  C07D273/01 ,  C07D261/14 ,  C07D207/08 ,  C07D209/20 ,  C07D211/14 ,  C07D213/75 ,  C07D213/81 ,  C07D233/64 ,  C07D235/06 ,  C07D241/44 ,  C07C311/19 ,  C07C317/46 ,  C07C271/28 ,  C07C275/28 ,  C07C233/83

摘要： The present invention pertains to a novel compound having anticancer activity, and a method for producing same, and more specifically, to a novel compound that exhibits excellent anticancer activity by inhibiting the expression of AIMP2-DX2, and a method for producing same. The compound represented by chemical formula 1 according to the present invention is highly effective in inhibiting the expression of AIMP2-DX2, and thus can be very advantageously used for the development of agents for treating various diseases, in particular cancer, caused by AIMP2-DX2.

公开(公告)号：US11312680B2

公开(公告)日：2022-04-26

申请号：US17406607

申请日：2021-08-19

申请人： King Abdulaziz University

发明人： Moustafa E. El-Araby ,  Abdelsattar M. Omar ,  Maan T. Khayat ,  Dhaval Shah ,  Martin K. Safo ,  Azizah M. Malebari ,  Farid Ahmed

IPC分类号： A61P35/00 ,  A61P35/02 ,  C07C233/64 ,  C07D295/192

摘要： Therapeutic compounds containing a phenyl core and amide link(s). Also described are pharmaceutical compositions incorporating the therapeutic compounds and a method for treating cancer with the compounds. These compounds are cytotoxic to stomach, colon, breast, and leukemia cancer cell lines via dual inhibition of Src kinases and tubulin.

公开(公告)号：US20220055983A1

公开(公告)日：2022-02-24

申请号：US17407276

申请日：2021-08-20

申请人： Purdue Research Foundation

发明人： Padinjaremadhom V. Ramachandran ,  Henry J. Hamann

IPC分类号： C07C231/02 ,  C07F5/02 ,  C07C233/65 ,  C07C233/58 ,  C07C233/05 ,  C07C233/08 ,  C07D295/192 ,  C07D213/82 ,  C07C323/41

摘要： The present invention generally relates to a process for selective and direct activation and subsequent amidation of aliphatic and aromatic carboxylic acids to afford an amide R3CONR1R2. That the process is capable of delivering gaseous or low-boiling point amines provides a major advantage over existing methodologies, which involves an intermediate of triacyloxyborane-amine complex [(R3CO2)3—B—NHR1R2]. This procedure readily produces primary, secondary, and tertiary amides, and is compatible with the chirality of the acid and amine involved. The preparation of known pharmaceutical molecules and intermediates has also been demonstrated.

公开(公告)号：US11230534B2

公开(公告)日：2022-01-25

申请号：US16672083

申请日：2019-11-01

申请人： Imago Biosciences, Inc.

发明人： Hugh Y. Rienhoff, Jr. ,  John M. McCall ,  Michael Clare ,  Cassandra Celatka ,  Amy E. Tapper

IPC分类号： A61K31/397 ,  C07D249/06 ,  C07C309/30 ,  A61K9/00 ,  A61K31/496 ,  C07D239/26 ,  A61K31/506 ,  C07D295/192 ,  A61K31/495 ,  C07D279/12 ,  A61K31/54 ,  C07D205/04 ,  C07D295/26 ,  C07D215/54 ,  C07C53/18 ,  C07D231/12 ,  C07D263/32 ,  A61K31/541 ,  C07B59/00 ,  C07D403/12 ,  A61K31/4192 ,  C07D401/12 ,  A61K31/454 ,  C07D249/08 ,  A61K31/4196 ,  C07D211/66 ,  A61K31/445 ,  C07D239/42 ,  C07D491/107 ,  C07D413/12 ,  A61K31/5377 ,  C07D498/08 ,  A61K31/5383 ,  C07D471/10 ,  A61K31/435 ,  C07D401/04 ,  A61K31/41 ,  C07D487/04 ,  A61K31/4162 ,  C07D487/08 ,  A61K31/4995 ,  A61K31/551 ,  C07D237/08 ,  A61K31/501 ,  A61K9/16 ,  A61K9/48 ,  A61K45/06 ,  A61P29/00 ,  A61P35/00 ,  A61P35/02 ,  A61P43/00

摘要： Disclosed herein are new compounds and compositions and their application as pharmaceuticals for the treatment of diseases. Methods of inhibition of KDM1A, methods of increasing gamma globin gene expression, and methods to induce differentiation of cancer cells in a human or animal subject are also provided for the treatment of diseases such as acute myelogenous leukemia.