公开(公告)号：US11110171B2

公开(公告)日：2021-09-07

申请号：US16956451

申请日：2018-12-21

Applicant: New York University

Inventor： Adam Mor ,  Ben Neel

IPC: C07K16/28 ,  A61K39/395 ,  A61P35/00 ,  G01N33/574 ,  G01N33/68 ,  A61K31/343 ,  A61K31/404 ,  A61K31/4412 ,  A61K31/4535 ,  A61K31/47 ,  A61K31/4704 ,  A61K31/497 ,  A61K38/46 ,  C12N15/113

Abstract: Provided are compositions and methods for identifying individuals with cancer who will benefit from PD-1 inhibitor therapy. The method comprises determining levels of signaling lymphocyte activation molecule-associated protein (SAP) in an individual and based on the SAP levels, determining if the individual is suitable for PD-1 inhibitor therapy. Also provided is a method of treatment of X-linked lymphoproliferative disease comprising administering to an individual PD-1 inhibitory therapy, with or without SHP2 inhibitors.

公开(公告)号：US20210236421A1

公开(公告)日：2021-08-05

申请号：US17233873

申请日：2021-04-19

Applicant: AMNEAL COMPLEX PRODUCTS RESEARCH LLC

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

IPC: 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

Abstract: 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

Applicant: Magenta Therapeutics Inc.

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

IPC: 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

Abstract: 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：US11065294B2

公开(公告)日：2021-07-20

申请号：US14891284

申请日：2014-05-15

Applicant: COMPREHENSIVE AND INTEGRATIVE MEDICINE INSTITUTE

Inventor： Joon Seok Byun ,  Sae Kwang Ku ,  Ki Cheul Sohn ,  Seung Mo Kim ,  Chang Hyeong Lee ,  Dae Sung Hyun ,  Jong Dae Kim ,  Sung Hwan Park ,  Min A. Kwak

IPC: A61K36/9068 ,  A61K31/138 ,  A61K36/232 ,  A61K36/484 ,  A61K36/725 ,  A61K36/00 ,  A61K31/44 ,  A61K31/4412 ,  A61K31/5377 ,  A61K36/28 ,  A61K36/53 ,  A61K36/65 ,  A61K36/752 ,  A61K36/756 ,  A61K36/88

Abstract: Provided is a composition for enhancing effects of an anticancer agent using an oriental medicine, jaeumganghwa-tang, bojungikgi-tang, or yukmijihwang-tang. More particularly, provided is a composition for treating a neoplastic disease by administering an anticancer agent into an individual, and administering an oriental medicine into the individual within 30 minutes. The composition remarkably reduces side effects occurring when the anticancer agent is administered alone by co-administration of the oriental medicine, reduces cytotoxicity, and has higher anticancer activity than that when the anticancer agent is administered alone.

公开(公告)号：US20210213027A1

公开(公告)日：2021-07-15

申请号：US17128634

申请日：2020-12-21

Applicant: Epizyme, Inc.

Inventor： Heike KEILHACK ,  Sarah K. KNUTSON

IPC: A61K31/5377 ,  A61K31/4412 ,  A61K31/4545 ,  A61P35/00 ,  A61K9/00

Abstract: The present disclosure relates to pharmaceutical compositions comprising inhibitor(s) of human histone methyltransferase EZH2, and methods of cancer therapy using the EZH2 inhibitor(s).

公开(公告)号：US11058690B2

公开(公告)日：2021-07-13

申请号：US16479531

申请日：2018-01-22

Applicant: BEIJING WEILANZHIYUAN MEDICAL TECHNOLOGY CO., LTD.

Inventor： Yuwen Cong

IPC: A61K31/539 ,  A61P29/00 ,  A61P25/14 ,  A61K31/122 ,  A61K31/155 ,  A61K31/165 ,  A61K31/216 ,  A61K31/22 ,  A61K31/357 ,  A61K31/366 ,  A61K31/40 ,  A61K31/404 ,  A61K31/415 ,  A61K31/4184 ,  A61K31/44 ,  A61K31/4412 ,  A61K31/47 ,  A61K31/473 ,  A61K31/505

Abstract: A use of an inhibitor of the cytochrome bc1 complex for preparing a pharmaceutical composition which treats diseases related to smooth muscle spasms, inflammatory diseases, and relieves pain.

公开(公告)号：US20210205284A1

公开(公告)日：2021-07-08

申请号：US17201190

申请日：2021-03-15

Applicant: CELGENE QUANTICEL RESEARCH, INC.

Inventor： Lynnie TRZOSS ,  Juan Manuel BETANCORT ,  Toufike KANOUNI ,  Michael Brennan WALLACE ,  Amogh BOLOOR

IPC: A61K31/4412 ,  A61P37/00 ,  A61P35/00 ,  A61P29/00

Abstract: The present embodiments relate to substituted heterocyclic derivative therapeutic compounds, compositions comprising said compounds, and the use of said compounds and compositions for epigenetic regulation by inhibition of bromodomain-mediated recognition of acetyl lysine regions of proteins, such as histones. Said compositions and methods are useful for the treatment of diseases mediated by aberrant cell signalling, such as inflammatory disorders, cancer and neoplastic disease. Particular compounds described herein exhibit selective inhibitory activity against CBP compared with BRD4.

公开(公告)号：US11026949B2

公开(公告)日：2021-06-08

申请号：US16562683

申请日：2019-09-06

Applicant: Epizyme, Inc. ,  Health Research, Inc.

Inventor： Heike Keilhack ,  Roberto Pili

IPC: A61K31/5377 ,  A61K31/404 ,  A61K31/444 ,  A61K31/506 ,  A61K31/517 ,  A61K31/4412 ,  A61K31/44 ,  A61K45/06 ,  A61P35/00 ,  A61K31/496

Abstract: The present disclosure relates to compositions comprising inhibitors of human histone methyltransferase EZH2 and one or more other therapeutic agents (such as tyrosine kinase inhibitors or VEGF/VEGFR inhibitors), particularly anticancer agents such as sunitinib, and methods of combination therapy for administering to subjects in need thereof for the treatment of cancer.

公开(公告)号：US11026937B2

公开(公告)日：2021-06-08

申请号：US16331622

申请日：2017-09-11

Applicant: PADLOCK THERAPEUTICS, INC.

Inventor： Rajesh Devraj ,  Gnanasambandam Kumaravel ,  Cristina Lecci ,  Pui Leng Loke ,  Mirco Meniconi ,  Nathaniel Julius Thomas Monck ,  Carl Leslie North ,  Mark Peter Ridgill ,  Heather Tye

IPC: C07D471/04 ,  A61K31/4375 ,  A61K31/47 ,  A61K31/4412 ,  A61K31/4709 ,  A61K31/5377 ,  C07D213/647 ,  C07D215/227 ,  C07D401/14 ,  C07D413/06

Abstract: The present invention provides compounds useful as inhibitors of PAD4, compositions thereof, and methods of treating PAD4-related disorders.

公开(公告)号：US10941115B2

公开(公告)日：2021-03-09

申请号：US16508253

申请日：2019-07-10

Applicant: Oxular Acquisitions Limited

Inventor： Thomas Matthew Baker ,  Matthew Colin Thor Fyfe ,  Geraint Jones ,  Stephen Malcolm Thom

IPC: C07D213/74 ,  C07F9/6512 ,  C07H19/048 ,  C07F9/59 ,  C07F9/6503 ,  A61K31/505 ,  A61K31/444 ,  A61K45/06 ,  A61K31/635 ,  A61K31/4375 ,  A61K31/7052 ,  A61K31/4412 ,  C07D405/12 ,  A61K31/541 ,  A61K31/551 ,  A61K31/553 ,  C07F9/58 ,  A61K31/44 ,  A61K31/506 ,  A61K31/675 ,  C07D213/80 ,  C07D401/12 ,  C07D239/47 ,  C07D413/12 ,  C07D453/02 ,  C07F9/6558 ,  C07H13/08 ,  C07H15/26 ,  A61K31/4439 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/706

Abstract: There are provided compounds of formula I, wherein R1A to R1E, R2 to R4, R5a, L and X1 to X3 have meanings given in the description, which compounds have anti-inflammatory activity (e.g. through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.