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公开(公告)号:US11564923B2
公开(公告)日:2023-01-31
申请号:US16757189
申请日:2018-10-11
申请人: Galapagos NV
发明人: Steven Emiel Van Der Plas , Oscar Mammoliti , Sébastien Laurent Xavier Martina , Pieter Isabelle Roger Claes , Ghjuvanni Petru Diunisu Coti , Denis Maurice Annoot , Miriam López Ramos , René Alexandre Galien , David Amantini , Reginald Christophe Xavier Brys
IPC分类号: A61K31/506 , A61P37/06 , A61P35/00 , A61K31/444 , A61K31/4545 , A61K31/496 , A61K31/501 , A61K31/5355 , C07D471/04 , C07D519/00
摘要: The present invention discloses compounds according to Formula I: Wherein R1, L1, R2, L2, R3, Cy, and the subscript n are as defined herein. The present invention relates to compounds, methods for their production, pharmaceutical compositions comprising the same, and methods of treatment using the same, for the prophylaxis and/or treatment of allergic diseases, inflammatory diseases, metabolic diseases, autoinflammatory diseases, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IFNα, IL12 and/or IL23 by administering the compound of the invention.
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公开(公告)号:US11555009B2
公开(公告)日:2023-01-17
申请号:US16490186
申请日:2018-03-01
发明人: Caiguang Yang , Yue Huang , Ze Dong , Tao Zhang , Hongjiao Xu
IPC分类号: C07C229/58 , A61P35/00 , C07D261/08 , A61K31/42 , A61K31/196 , C07D231/12 , A61K31/415 , C07D213/38 , A61K31/4418 , C07D333/20 , A61K31/381 , C07D239/26 , A61K31/505 , C07D333/40 , C07D239/42 , C07D211/70 , C07D209/14 , A61K31/404 , C07D233/64 , A61K31/4164 , C07D257/04 , A61K31/41 , C07D407/12 , A61K31/422 , A61K31/4245 , C07D401/12 , A61K31/4439 , A61K31/5355 , C07C227/16
摘要: The invention provides 2-(substituted phenylhetero) aromatic formate FTO inhibitors, a preparation method thereof, and applications thereof. Specifically, disclosed in the present invention are a 2-(substituted phenylhetero) aromatic formate compound represented by the following formula (I), and a pharmaceutically acceptable salt, a hydrate or a solvate thereof, which can be used as an FTO targeting inhibitor for treating diseases associated with FTO targets, including obesity, metabolic syndrome (MS), type 2 diabetes (T2D), Alzheimer's diseases, and cancers such as breast cancers, small-cell lung cancers, human bone marrow rhabdomyosarcoma, pancreatic cancer, malignant glioblastoma and the like.
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公开(公告)号:US11529344B2
公开(公告)日:2022-12-20
申请号:US16762388
申请日:2018-11-09
申请人: Pfizer Inc.
IPC分类号: A61K31/4725 , A61P35/00 , A61K33/243 , A61K31/357 , A61K31/4412 , A61K31/4433 , A61K31/4545 , A61K31/496 , A61K31/501 , A61K31/5355 , A61K39/395 , A61K45/06
摘要: This invention relates to combination therapies comprising an EZH2 inhibitor and a chemotherapeutic agent, and associated pharmaceutical compositions, methods of treatment, and pharmaceutical uses.
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公开(公告)号:US11446315B2
公开(公告)日:2022-09-20
申请号:US16344974
申请日:2017-11-01
IPC分类号: A61K38/08 , A61K38/17 , A61K47/68 , A61K31/69 , A61P35/02 , A61K31/5355 , A61K38/07 , C07K7/06 , C07K14/705 , C07K16/28 , A61P35/00 , C07F5/02 , C07F5/04 , C07K16/00 , A61K38/00 , A61K38/05
摘要: CD47− disease cells such as cancer cells are treated using a combination of CD47 blockade drug and a proteasome inhibitor. The anti-cancer effect of one drug enhances the 5 anti-cancer effect of the other. Specific combinations include SIRPαFc as CD47 blockade drug, and one of bortezomib, ixazomib and carfilzomib as proteasome inhibitor. These combinations are useful particularly to treat blood cancers including lymphomas, leukemias and myelomas.
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公开(公告)号:US11426404B2
公开(公告)日:2022-08-30
申请号:US15930606
申请日:2020-05-13
申请人: AMGEN INC.
IPC分类号: A61K31/505 , A61P35/00 , A61K9/00 , A61K31/53 , A61K31/5355 , A61K39/00
摘要: Provided herein are methods of administering a KRAS G12C inhibitor to a cancer subject.
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公开(公告)号:US11247971B2
公开(公告)日:2022-02-15
申请号:US17160868
申请日:2021-01-28
申请人: THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES , VANDERBILT UNIVERSITY , The UAB Research Foundation , The Trustees of the University of Pennsylvania
发明人: David J. Maloney , Alex Gregory Waterson , Ganesh Rai Bantukallu , Kyle Ryan Brimacombe , Plamen Christov , Chi V. Dang , Victor Darley-Usmar , Xin Hu , Ajit Jadhav , Somnath Jana , Kwangho Kim , Jennifer L. Kouznetsova , William J. Moore , Bryan T. Mott , Leonard M. Neckers , Anton Simeonov , Gary Allen Sulikowski , Daniel Jason Urban , Shyh Ming Yang
IPC分类号: C07D231/20 , C07D231/38 , C07D401/04 , C07D403/04 , C07D403/06 , C07D409/04 , C07D413/04 , C07D417/04 , C07D417/14 , C07D471/04 , C07D495/04 , C07D495/14 , A61K31/415 , A61K31/4155 , A61K31/4178 , A61K31/422 , A61K31/427 , A61K31/437 , A61K31/454 , A61K31/496 , A61K31/501 , A61K31/506 , A61K31/519 , A61K31/5355 , A61K31/4439 , A61K45/06
摘要: Provided is a compound of formula (I), in which Ar1, R1, U, V, W, X, and p are as described herein. Also provided are methods of using a compound of formula (I), including a method of treating cancer, a method of treating a patient with cancer cells resistant to an anti-cancer agent, and a method of inhibiting lactate dehydrogenase A (LDHA) and/or lactate dehydrogenase B (LDHB) activity in a cell.
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公开(公告)号:US11104670B2
公开(公告)日:2021-08-31
申请号:US16654031
申请日:2019-10-16
IPC分类号: A61K31/5355 , A61P25/00 , C07D413/06 , A61K45/06
摘要: Disclosed are 4-pyrimidin-5-ylmethyl-morpholines of formula A and pharmaceutically acceptable salts thereof, wherein R1 and R2 are defined herein. Also disclosed are processes for their preparation, pharmaceutical compositions containing the compounds, and their use in therapy, particularly in the treatment or prevention of conditions having an association with NR2B negative allosteric modulating properties.
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公开(公告)号:US20210253568A1
公开(公告)日:2021-08-19
申请号:US16973514
申请日:2019-06-11
IPC分类号: C07D471/04 , A61K45/06 , A61K33/00 , A61K9/00 , A61K31/4725 , A61K31/444 , A61K31/506 , C07D487/04 , A61K31/519 , A61K31/5355 , C07D519/00
摘要: The invention relates to compounds of formula I inhibiting Rho Kinase that are azaindole derivatives, methods of preparing such compounds, pharmaceutical compositions containing them and therapeutic use thereof. Particularly the compounds of the invention may be useful in the treatment of many disorders associated with ROCK enzymes mechanisms, such as pulmonary diseases including asthma, chronic obstructive pulmonary disease (COPD), idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH).
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公开(公告)号:US20210236487A1
公开(公告)日:2021-08-05
申请号:US17051836
申请日:2019-05-01
发明人: Jamille M. SHAMMO , Lydia USHA
IPC分类号: A61K31/501 , A61K31/519 , A61K45/06 , A61P35/00 , A61K31/55 , A61K31/4439 , A61K31/5025 , A61K31/502 , A61K31/407 , A61K31/496 , A61K31/5355 , A61K31/28 , A61K31/5517 , G01N33/82
摘要: Methods of treating cancer in a subject and compositions are provided. The methods include administering a therapeutically effective amount of a poly (ADP ribose) polymerase (PARP) inhibitor to the subject in need thereof and administering a therapeutically effective amount of a folic acid supplement to the subject. Also described herein are methods for identifying a subject having cancer and having an elevated folate receptor expression level relative to a folate receptor expression level in a subject free of cancer and administering a therapeutically effective amount of a PARP inhibitor to the subject having the elevated folate receptor level. Also described herein are compositions including a PARP inhibitor and a folic acid supplement.
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公开(公告)号:US20210171653A1
公开(公告)日:2021-06-10
申请号:US17112862
申请日:2020-12-04
申请人: Sanofi-Aventis U.S. LLC , Sanofi
发明人: Marie-Laure RISSE , Gaelle ASSET
IPC分类号: C07K16/28 , A61P35/00 , A61K31/573 , A61K31/5355
摘要: The present disclosure provides methods for treating multiple myeloma (such as refractory multiple myeloma or relapsed and refractory multiple myeloma) in an individual who received one to three prior therapies (or prior lines of therapy) for multiple myeloma. The methods comprise administering to the individual an anti-CD38 antibody, carfilzomib, and dexamethasone.
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