公开(公告)号：US20230210862A1

公开(公告)日：2023-07-06

申请号：US18147030

申请日：2022-12-28

申请人： INDIAN INSTITUTE OF TECHNOLOGY KANPUR

发明人： Bushra Ateeq ,  Sakshi Goel

IPC分类号： A61K31/551 ,  A61K31/4166 ,  A61P13/08 ,  A61P35/00

CPC分类号： A61K31/551 ,  A61K31/4166 ,  A61P13/08 ,  A61P35/00

摘要： A formulation and method for treating prostate cancer is provided. The method includes use of bromodomain and extra-terminal domain inhibitors (BETi) or combination of BETi and anti-androgen drug to therapeutically target DLX1-positive advanced-stage prostate cancer patients. The formulation for treating prostate cancer relates to disrupting ERG/AR transcriptional circuitry with BETi in combination with anti-androgen drug to attenuate DLX1 expression and its downstream oncogenic effects. The BETi and the combination of BETi and anti-androgen drug yields 60% of tumor regression and remarkable reduction in distant metastases in the preclinical immunodeficient mice bearing DLX1-positive tumors.

公开(公告)号：US20230174562A1

公开(公告)日：2023-06-08

申请号：US17923831

申请日：2021-05-07

申请人： TONIX PHARMACEUTICALS, INC. ,  TONIX PHARMACEUTICALS HOLDING CORP.

发明人： Philip S. Schein ,  Darryl C. Rideout

IPC分类号： C07F9/165 ,  A61K45/06 ,  A61P39/00 ,  A61K31/661 ,  C07D243/08 ,  A61K31/551 ,  C07D241/04 ,  A61K31/495 ,  C07D243/10 ,  C07D245/02 ,  A61K31/395 ,  C07D245/04 ,  C07D487/04 ,  A61K31/4985 ,  C07C53/18 ,  C07D241/38 ,  A61K31/498 ,  C07F9/6571 ,  A61K31/675 ,  C07C323/25 ,  A61K31/145

CPC分类号： C07F9/1651 ,  A61K45/06 ,  A61P39/00 ,  A61K31/661 ,  C07D243/08 ,  A61K31/551 ,  C07D241/04 ,  A61K31/495 ,  C07D243/10 ,  C07D245/02 ,  A61K31/5545 ,  C07D245/04 ,  C07D487/04 ,  A61K31/4985 ,  C07C53/18 ,  C07D241/38 ,  A61K31/498 ,  C07F9/657118 ,  A61K31/675 ,  C07C323/25 ,  A61K31/145 ,  C07B2200/13

摘要： The present disclosure relates to prodrugs, double prodrugs, derivatives and analogues of 3-(methylamino)-2-((methy-lamino)methyl)propane-1-thiol. Their use as radio- and chemo-protectors is also described.

公开(公告)号：US20230158071A1

公开(公告)日：2023-05-25

申请号：US17311466

申请日：2019-12-09

申请人： CRAGE medical Co., Limited

发明人： Zonghai LI ,  Ruixin SUN

IPC分类号： A61K35/17 ,  A61K31/454 ,  A61K31/5025 ,  A61K31/55 ,  A61K31/551 ,  C07K14/705 ,  C07K16/28 ,  A61K45/06

CPC分类号： A61K35/17 ,  A61K31/454 ,  A61K31/5025 ,  A61K31/55 ,  A61K31/551 ,  C07K14/70517 ,  C07K14/70521 ,  C07K16/2863 ,  A61K45/06 ,  C07K2319/03 ,  C12N2510/00

摘要： Provided is a method for tumor treatment, comprising administering immune effector cells and a PARP inhibitor to an individual suffering from a tumor, the immune effector cell expresses a receptor for identifying a tumor antigen. Further provided is a kit for tumor treatment.

公开(公告)号：US11654147B2

公开(公告)日：2023-05-23

申请号：US17340589

申请日：2021-06-07

申请人： The Brigham and Women's Hospital, Inc. ,  The United States of America, as Represented by the Secretary, Department of Health and Human Services

发明人： Paul B. Yu ,  Wenwei Huang ,  Philip Edward Sanderson ,  Jian-Kang Jiang ,  Khalida Shamim ,  Wei Zheng ,  Xiuli Huang ,  Gregory Tawa ,  Arthur Lee ,  Asaf Alimardanov ,  Junfeng Huang

IPC分类号： A61K31/519 ,  A61P19/08 ,  A61K31/5377 ,  A61K31/551 ,  A61K31/675 ,  A61K45/06 ,  C07D487/04 ,  C07D519/00 ,  C07F9/6561

CPC分类号： A61K31/519 ,  A61K31/5377 ,  A61K31/551 ,  A61K31/675 ,  A61K45/06 ,  A61P19/08 ,  C07D487/04 ,  C07D519/00 ,  C07F9/6561

摘要： The present invention provides small-molecule inhibitors of BMP signaling and compositions and methods for inhibiting BMP signaling. These compounds and compositions may be used to modulate cell growth, differentiation, proliferation, and apoptosis, and thus may be useful for treating diseases or conditions associated with BMP signaling, including inflammation, cardiovascular disease, hematological disease, cancer, and bone disorders, as well as for modulating cellular differentiation and/or proliferation. These compounds and compositions may also be used to treat subjects with Sjögren's syndrome, or diffuse intrinsic pontine glioma (DIPG).

公开(公告)号：US20190240198A1

公开(公告)日：2019-08-08

申请号：US15888962

申请日：2018-02-05

申请人： Dean G. Tang ,  Xin Chen

发明人： Dean G. Tang ,  Xin Chen

IPC分类号： A61K31/4166 ,  A61P35/00

CPC分类号： A61K31/4166 ,  A61K31/437 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/551 ,  A61K2300/00 ,  A61P35/00

摘要： The present invention is directed to a formulation for treating cancer comprising an androgen receptor signaling inhibitor and a B-cell-lymphoma-2 inhibitor, which may further comprising a Bromodomain-and-Extra-Terminal protein inhibitor or a phosphoinositide 3-kinase inhibitor.

公开(公告)号：US20190233406A1

公开(公告)日：2019-08-01

申请号：US16246068

申请日：2019-01-11

申请人： Merck Sharp & Dohme Corp.

发明人： Thomas J. Greshock ,  James Mulhearn ,  Junying Zheng ,  Ronald M. Kim ,  Ting Zhang ,  Anthony J. Roecker ,  Walter Won ,  Philippe Nantermet ,  Rajan Anand ,  Gang Zhou ,  Deping Wang ,  Liangqin Guo

IPC分类号： C07D417/12 ,  A61K31/426 ,  A61K31/433 ,  A61K31/427 ,  A61K31/551 ,  C07D277/52 ,  C07D285/08 ,  A61K45/06

CPC分类号： C07D417/12 ,  A61K31/426 ,  A61K31/427 ,  A61K31/433 ,  A61K31/551 ,  A61K45/06 ,  C07D277/52 ,  C07D285/08 ,  A61K2300/00

摘要： Disclosed are compounds of Formula A, or a salt thereof: wherein R1, R2, and E are defined herein, which compounds have properties for inhibiting Nav 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula A or their salts, and methods of treating pain disorders, cough, and itch using the same.

公开(公告)号：US20190216764A1

公开(公告)日：2019-07-18

申请号：US16273986

申请日：2019-02-12

申请人： KING FAHD UNIVERSITY OF PETROLEUM AND MINERALS

发明人： Mohammed Yagoub Jomaa ,  Anvarhusein A. Isab

IPC分类号： A61K31/282 ,  A61K31/505 ,  C07F15/00 ,  A61K31/095 ,  A61K33/24

CPC分类号： A61K31/282 ,  A61K31/095 ,  A61K31/4164 ,  A61K31/505 ,  A61K31/551 ,  A61K33/24 ,  C07F15/0013

摘要： A method for treating a proliferative disease, disorder, or condition comprising administering a cis-diamine platinum(II) thione complex. A cis-diamine platinum(II) thione complex and compositions containing it.

公开(公告)号：US20190209560A1

公开(公告)日：2019-07-11

申请号：US16178678

申请日：2018-11-02

申请人： eFFECTOR Therapeutics, Inc.

发明人： Siegfried H. Reich ,  Paul A. Sprengeler ,  Stephen E. Webber ,  Alan X. Xiang ,  Justin T. Ernst

IPC分类号： A61K31/506 ,  A61K31/551 ,  A61K31/52 ,  A61K31/519 ,  C07D519/00 ,  C07D495/20 ,  C07D471/04 ,  C07D471/20 ,  C07D471/10 ,  C07D487/04 ,  C07D473/34 ,  C07D491/20

CPC分类号： A61K31/506 ,  A61K31/519 ,  A61K31/52 ,  A61K31/551 ,  C07D471/04 ,  C07D471/10 ,  C07D471/20 ,  C07D473/34 ,  C07D487/04 ,  C07D491/20 ,  C07D495/20 ,  C07D519/00

摘要： The present invention relates to compounds according to Formula (I): or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4a, R4b, R5, R6, R7, R8, W1, W2, Y and n are as defined herein. Also described are pharmaceutically acceptable compositions of Formula I compounds as well as methods for utilizing the compounds of Formula I and the pharmaceutically acceptable compositions of Formula I compounds as inhibitors of Mnk as well as therapeutics for the treatment of diseases such as cancer.

公开(公告)号：US20190105327A1

公开(公告)日：2019-04-11

申请号：US16041237

申请日：2018-07-20

申请人： Essentialis, Inc.

发明人： Neil M. COWEN

IPC分类号： A61K31/549 ,  A61K38/27 ,  A61K9/00 ,  A61K9/50 ,  A61K9/20 ,  C07D285/22 ,  C07D285/18 ,  A61K45/06 ,  A61K31/137 ,  A61K31/155 ,  A61K31/551

CPC分类号： A61K31/549 ,  A61K9/00 ,  A61K9/0004 ,  A61K9/2054 ,  A61K9/5026 ,  A61K9/5042 ,  A61K9/5047 ,  A61K31/137 ,  A61K31/155 ,  A61K31/551 ,  A61K38/27 ,  A61K45/06 ,  A61K2300/00 ,  C07D285/18 ,  C07D285/22

摘要： Provided are immediate or prolonged administration of certain potassium ATP (KATP) channel openers, optionally in combination with growth hormone, to a subject to achieve novel pharmacodynamic, pharmacokinetic, therapeutic, physiological, metabolic and compositional outcomes in the treatment of diseases or conditions involving KATP channels. Also provided are pharmaceutical formulations, methods of administration and dosing of KATP channel openers that achieve these outcomes and reduce the incidence of adverse effects in treated individuals. Further provided are methods of co-administering KATP channel openers with other drugs (e.g., in combination with growth hormone) to treat diseases of humans and animals (e.g., Prader-Willi Syndrome (PWS), Smith-Magenis syndrome (SMS), and the like.

公开(公告)号：US20190010143A1

公开(公告)日：2019-01-10

申请号：US15719867

申请日：2017-09-29

申请人： Beijing Tide Pharmaceutical Co., Ltd.

发明人： Yanping ZHAO ,  Hongjun WANG ,  Gong LI ,  Yuanyuan JIANG ,  Xiang LI ,  Liying ZHOU ,  Yanan LIU

IPC分类号： C07D405/14 ,  C07D409/14 ,  C07D403/14 ,  C07D491/048 ,  C07D495/04 ,  C07D487/04 ,  C07D403/04 ,  C07D417/14 ,  C07D498/04 ,  C07D513/04 ,  C07D413/14 ,  C07D471/04 ,  C07D401/14 ,  C07D471/08 ,  C07D471/10 ,  C07D487/10

CPC分类号： C07D405/14 ,  A61K31/343 ,  A61K31/351 ,  A61K31/357 ,  A61K31/381 ,  A61K31/397 ,  A61K31/404 ,  A61K31/4155 ,  A61K31/416 ,  A61K31/423 ,  A61K31/425 ,  A61K31/428 ,  A61K31/433 ,  A61K31/4412 ,  A61K31/4439 ,  A61K31/4465 ,  A61K31/496 ,  A61K31/501 ,  A61K31/506 ,  A61K31/519 ,  A61K31/53 ,  A61K31/5375 ,  A61K31/55 ,  A61K31/551 ,  A61K31/5513 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/08 ,  C07D471/10 ,  C07D487/04 ,  C07D487/10 ,  C07D491/04 ,  C07D491/048 ,  C07D495/04 ,  C07D498/04 ,  C07D513/04

摘要： The present invention relates to a Rho-associated protein kinase inhibitor of Formula (I), a pharmaceutical composition comprising the same, a preparation method thereof, and use thereof for the prevention or treatment of a disease mediated by the Rho-associated protein kinase (ROCK).