公开(公告)号：US20210393549A1

公开(公告)日：2021-12-23

申请号：US17274175

申请日：2019-09-07

申请人： Tan WEN

发明人： Tan WEN

IPC分类号： A61K31/137 ,  A61K31/27 ,  A61K31/138 ,  A61K31/538 ,  A61K31/4704 ,  A61K31/55 ,  A61K31/655 ,  A61K31/573 ,  A61K31/407 ,  A61K31/545 ,  A61K31/427 ,  A61K31/43 ,  A61K31/345 ,  A61K31/65 ,  A61K31/421 ,  A61K31/397 ,  A61K31/4439 ,  A61K39/395 ,  A61P37/06 ,  A61P17/06

摘要： This invention disclosed a new use of optically pure R-enantiomer of adrenergic β2 agonists including R-salbutamol, R-terbutaline, R-clenbuterol and R-bambuterol for treatment of inflammatory bowel disease and its extra intestinal manifestations including skin diseases.

公开(公告)号：US20210353569A1

公开(公告)日：2021-11-18

申请号：US17383131

申请日：2021-07-22

申请人： OMEICOS Therapeutics GmbH ,  Max Delbrück-Centrum für Molekulare Medizin

发明人： Robert Fischer ,  Wolf-Hagen Schunck ,  Dominik Müller ,  Tim Wesser ,  Anne Konkel ,  Janine Lossie

IPC分类号： A61K31/165 ,  A61K31/192 ,  A61K31/22 ,  A61K31/341 ,  A61K31/351 ,  A61P29/00 ,  A61K31/4196 ,  A61K31/421 ,  A61K31/5375 ,  A61P27/02 ,  A61K31/40

摘要： The present invention relates to compounds according to general formula (I) which are metabolically robust analogues of bioactive lipid mediators derived from omega-3 polyunsaturated fatty acids (n-3 PUFAs) for use in treating or reducing the risk of developing or preventing: (i) neovascularization and/or (ii) inflammatory disorder, in particular, ophthalmic disorders associated with neovascularization and/or inflammation.

公开(公告)号：US20210299107A1

公开(公告)日：2021-09-30

申请号：US17330386

申请日：2021-05-25

申请人： THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK

发明人： Brent R. Stockwell ,  Arie Zask ,  Hui Tan ,  Jacob Daniels

IPC分类号： A61K31/4245 ,  C07D271/10 ,  C07D263/32 ,  C07C229/60 ,  C07C233/65 ,  C07D295/13 ,  C07D213/74 ,  C07D413/04 ,  C07D213/80 ,  C07D413/12 ,  A61P39/06 ,  A61P31/06 ,  A61K31/421 ,  A61K31/245 ,  A61K31/166 ,  A61K31/5375 ,  A61K31/44 ,  A61K31/4439

摘要： The present disclosure provides, inter alia, a compound having the structure: Also provided are compositions containing a pharmaceutically acceptable carrier and one or more compounds according to the present disclosure. Further provided are methods for treating or ameliorating the effects of an excitotoxic disorder in a subject, methods of modulating ferroptosis in a subject, methods of reducing reactive oxygen species (ROS) in a cell, methods for treating or ameliorating the effects of a neurodegenerative disease, methods for alleviating side effects in a subject undergoing radiotherapy and/or immunotherapy, and methods for treating or ameliorating the effects of an infection associated with ferroptosis in a subject.

公开(公告)号：US11124502B2

公开(公告)日：2021-09-21

申请号：US16739525

申请日：2020-01-10

申请人： THERAVANCE BIOPHARMA R&D IP, LLC

发明人： Melissa Fleury ,  Adam D. Hughes

IPC分类号： C07D405/12 ,  A61K31/415 ,  A61K31/4192 ,  A61K31/42 ,  A61K31/421 ,  A61K45/06 ,  C07D231/14 ,  C07D231/20 ,  C07D261/18 ,  C07D263/38 ,  C07D249/04

摘要： In one aspect, the invention relates to compounds having the formula: where X, Ra, Rb, R2, and R7 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds are prodrugs of compounds having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.

公开(公告)号：US20210269399A1

公开(公告)日：2021-09-02

申请号：US17038179

申请日：2020-09-30

申请人： Calico Life Sciences LLC ,  AbbVie Inc.

发明人： Carmela Sidrauski ,  Marina Pliushchev ,  Jennifer M. Frost ,  Lawrence A. Black ,  Xiangdong Xu ,  Ramzi Farah Sweis ,  Lei Shi ,  Qingwei Zhang ,  Yunsong Tong ,  Charles W. Hutchins ,  SeungWon Chung ,  Michael J. Dart

IPC分类号： C07D213/42 ,  C07D231/12 ,  C07D237/08 ,  C07D239/34 ,  C07D241/12 ,  C07D471/04 ,  C07D261/08 ,  C07D263/32 ,  C07D277/28 ,  C07D209/14 ,  C07C235/22 ,  C07D213/40 ,  C07D213/64 ,  C07D307/52 ,  C07D271/07 ,  A61K31/18 ,  A61K31/197 ,  A61K31/341 ,  A61K31/381 ,  A61K31/4045 ,  A61K31/415 ,  A61K31/417 ,  A61K31/42 ,  A61K31/421 ,  A61K31/4245 ,  A61K31/426 ,  A61K31/44 ,  A61K31/4439 ,  A61K31/4965 ,  A61K31/50 ,  A61K31/505 ,  C07C311/16 ,  C07C323/09 ,  C07D213/89 ,  C07D235/00 ,  C07D271/10 ,  C07D307/36 ,  C07D333/20

摘要： Provided herein are compounds, compositions, and methods useful for modulating the integrated stress response (ISR) and for treating related diseases; disorders and conditions.

公开(公告)号：US20210236421A1

公开(公告)日：2021-08-05

申请号：US17233873

申请日：2021-04-19

申请人： AMNEAL COMPLEX PRODUCTS RESEARCH LLC

发明人： Kanji Meghpara ,  Jaydeep Vaghashiya ,  Navnit H. Shah ,  Dipen Desai ,  Wantanee Phuapradit ,  Harpreet Kaur Sandhu ,  Siva Ram Kiran Vaka ,  Namdev B. Shelke ,  Ashish Chatterji

IPC分类号： A61K9/00 ,  A61K9/28 ,  A61K31/195 ,  A61K31/403 ,  A61K31/421 ,  A61K31/4412 ,  A61K9/46 ,  A61K31/198 ,  A61K31/404 ,  A61K31/4166 ,  A61K31/4425 ,  A61K47/32 ,  A61K47/34 ,  A61K47/38

摘要： The present disclosure is directed to floating gastroretentive dosage forms with prolonged gastric residence time. The disclosure also provides rapidly expanding sustained release or combined immediate release and sustained release formulations comprising drugs that require targeted release in the proximal gastrointestinal tract for maximum therapeutic benefit. The rapidly expanding floating gastroretentive dosage forms comprise a permeable elastic membrane providing desired characteristics for drug release and mechanical strength to maintain tablet integrity.

公开(公告)号：US20210220408A1

公开(公告)日：2021-07-22

申请号：US17273510

申请日：2019-09-04

申请人： Magenta Therapeutics Inc.

发明人： Anthony BOITANO ,  Michael COOKE ,  Kevin A. GONCALVES ,  Megan HOBAN

IPC分类号： A61K35/28 ,  C07D295/135 ,  C07D261/08 ,  C07D405/12 ,  C07D249/06 ,  C07D487/04 ,  C07C255/60 ,  C07D498/04 ,  C07D513/04 ,  C07D237/20 ,  C07D231/56 ,  C07D237/24 ,  C07D249/12 ,  C07D209/44 ,  C07D277/28 ,  C07D275/04 ,  C07C233/81 ,  C07D213/75 ,  C07D207/34 ,  C07D495/04 ,  C07D215/38 ,  C07D417/12 ,  C07D235/18 ,  C07D307/91 ,  C07D495/14 ,  C07D471/04 ,  C07D471/14 ,  C07D409/12 ,  C07D413/12 ,  C07D213/82 ,  C07D249/04 ,  C07D417/04 ,  C07D401/14 ,  A61K31/5375 ,  A61K31/277 ,  A61K31/42 ,  A61K31/443 ,  A61K31/519 ,  A61K31/4192 ,  A61K31/437 ,  A61K31/501 ,  A61K31/50 ,  A61K31/416 ,  A61K31/429 ,  A61K31/4196 ,  A61K31/4035 ,  A61K31/426 ,  A61K31/428 ,  A61K31/167 ,  A61K31/4162 ,  A61K31/44 ,  A61K31/415 ,  A61K31/47 ,  A61K31/427 ,  A61K31/454 ,  A61K31/4184 ,  A61K31/343 ,  A61K31/4365 ,  A61K31/381 ,  A61K31/4155 ,  A61K31/4436 ,  A61K31/423 ,  A61K31/55 ,  A61K31/421 ,  A61K31/425 ,  A61K31/4412 ,  A61K31/505 ,  A61K31/422 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4439 ,  A61K31/4704 ,  A61K31/4709 ,  A61K31/5377 ,  A61K31/366 ,  C12N5/0789 ,  G01N33/50 ,  A61K45/06

摘要： The disclosure relates to aryl hydrocarbon receptor antagonists as well as methods of modulating aryl hydrocarbon receptor activity and expanding hematopoietic stem cells by culturing hematopoietic stem or progenitor cells in the presence of these agents. Additionally, the disclosure provides methods of treating various pathologies, such as cancer, by administration of these aryl hydrocarbon receptor antagonists. Additionally, the disclosure provides methods of treating various pathologies in a patient by administration of expanded hematopoietic stem cells. The disclosure further provides kits containing aryl hydrocarbon receptor antagonists that can be used for the expansion of hematopoietic stem cells. The disclosure further relates to pharmaceutical compositions comprising the compounds and methods of treating or preventing a disease in which aryl hydrocarbon receptor plays a role.

公开(公告)号：US20210169838A1

公开(公告)日：2021-06-10

申请号：US17115825

申请日：2020-12-09

申请人： Stichting Katholieke Universiteit

发明人： Tom Johan Joseph Schirris ,  Tina Ritschel ,  Floris Petrus Johannes Theodorus Rutjes ,  Johannes Albertus Maria Smeitink ,  François Gérard Marie Russel

IPC分类号： A61K31/215 ,  A61K31/4164 ,  A61P25/28 ,  A61K31/4025 ,  A61K31/505 ,  A61K31/381 ,  A61P9/10 ,  A61K31/366 ,  A61K31/426 ,  A61K31/421 ,  A61K31/404 ,  A61P3/06 ,  A61K31/16 ,  A61K31/365 ,  A61K45/06

摘要： The present invention relates to the field of medicine, specifically the field of treatment and prevention of cardiovascular diseases.

公开(公告)号：US20210121476A1

公开(公告)日：2021-04-29

申请号：US17140704

申请日：2021-01-04

申请人： The United States of America,as represented by the Secretary,Department of Health and Human Services

发明人： Sanjay A. Desai ,  Ajay D. Pillai

IPC分类号： A61K31/553 ,  A61K31/165 ,  A61K31/4155 ,  A61K31/423 ,  A61K31/4245 ,  A61K31/433 ,  A61K31/4355 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/4741 ,  A61K31/4745 ,  A61K31/50 ,  A61K31/554 ,  A61K45/06 ,  C07D403/08 ,  C07D498/04 ,  C07D263/57 ,  C07D281/16 ,  C07D413/14 ,  C07D417/06 ,  C07D491/048 ,  C07D513/04 ,  A61K31/421

摘要： Disclosed are inhibitors of the plasmodial surface anion channel (PSAC) inhibitors and the use thereof in treating or preventing malaria in an animal such as a human, comprising administering an effective amount of an inhibitor or a combination of inhibitors. An example of such an inhibitor is a compound of formula I, or a pharmaceutically acceptable salt thereof, wherein R1 to R7 are as described herein.

公开(公告)号：US10947207B2

公开(公告)日：2021-03-16

申请号：US16323033

申请日：2017-08-04

申请人： THE REGENTS OF THE UNIVERSITY OF CALIFORNIA

发明人： Mohammad Parvez Alam ,  Varghese John ,  Patricia Spilman ,  Kanagasabai Vadivel

IPC分类号： C07D277/42 ,  C07D263/48 ,  C07D413/04 ,  C07D417/04 ,  C07D487/08 ,  C07D263/28 ,  A61K31/4439 ,  A61K31/421 ,  A61K31/506 ,  A61K31/426 ,  A61P25/00

摘要： There are provided, inter alia, compounds and methods useful for the treatment of neurological conditions, such as neurological disorders and neurodegenerative diseases, including Alzheimer's Disease.