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![SUBSTITUTED 1H-PYRAZOLO[4,3-C]PYRIDINES AND DERIVATIVES AS EGFR INHIBITORS](/abs-image/US/2024/10/31/US20240358688A1/abs.jpg.150x150.jpg)
公开(公告)号：US20240358688A1
公开(公告)日：2024-10-31
申请号：US18756533
申请日：2024-06-27
发明人： Harald ENGELHARDT , Mark PETRONCZKI , Juergen RAMHARTER , Ulrich REISER , Heinz STADTMUELLER , Dirk SCHARN , Tobias WUNBERG
IPC分类号： A61K31/437 , A61K31/4545 , A61K31/496 , A61K31/4995 , A61K31/5377 , A61K31/5386 , A61K31/541 , A61K31/553 , A61P35/00 , C07D211/04 , C07D519/00
CPC分类号： A61K31/437 , A61K31/4545 , A61K31/4995 , A61K31/553 , A61P35/00 , C07D211/04 , C07D519/00 , A61K31/496 , A61K31/5377 , A61K31/5386 , A61K31/541
摘要： The present invention encompasses compounds of formula (I)
wherein the groups R1 to R4 and X1 to X5 have the meanings given in the claims and specification, their use as inhibitors of mutant EGFR, pharmaceutical compositions which contain compounds of this kind and their use as medicaments/medical uses, especially as agents for treatment and/or prevention of oncological diseases.-
![Substituted 1H-pyrazolo[4,3-c]pyridines and derivatives as EGFR inhibitors](/abs-image/US/2024/08/20/US12064421B2/abs.jpg.150x150.jpg)
公开(公告)号：US12064421B2
公开(公告)日：2024-08-20
申请号：US17514145
申请日：2021-10-29
发明人： Harald Engelhardt , Mark Petronczki , Juergen Ramharter , Ulrich Reiser , Heinz Stadtmueller , Dirk Scharn , Tobias Wunberg
IPC分类号： C07D211/04 , A61K31/437 , A61K31/4545 , A61K31/4995 , A61K31/553 , A61P35/00 , C07D519/00 , A61K31/496 , A61K31/5377 , A61K31/5386 , A61K31/541
CPC分类号： A61K31/437 , A61K31/4545 , A61K31/4995 , A61K31/553 , A61P35/00 , C07D211/04 , C07D519/00 , A61K31/496 , A61K31/5377 , A61K31/5386 , A61K31/541
摘要： The present invention encompasses compounds of formula (I)
wherein the groups R1 to R4 and X1 to X5 have the meanings given in the claims and specification, their use as inhibitors of mutant EGFR, pharmaceutical compositions which contain compounds of this kind and their use as medicaments/medical uses, especially as agents for treatment and/or prevention of oncological diseases.-
公开(公告)号：US20240262821A1
公开(公告)日：2024-08-08
申请号：US18557852
申请日：2022-05-06
发明人： Peter Ray , Anthony Bradley , Simon Richards , Catarina Santos , Jeremy Besnard , Jérôme Meneyrol , Virginie Suchaud
IPC分类号： C07D471/04 , A61K31/437 , A61K31/4545 , A61K31/496 , A61K31/498 , A61K31/4985 , A61K31/4995 , A61K31/506 , A61K31/519 , A61K31/5383 , A61K31/551 , C07D487/04 , C07D498/04 , C07D519/00
CPC分类号： C07D471/04 , A61K31/437 , A61K31/4545 , A61K31/496 , A61K31/498 , A61K31/4985 , A61K31/4995 , A61K31/506 , A61K31/519 , A61K31/5383 , A61K31/551 , C07D487/04 , C07D498/04 , C07D519/00
摘要： Disclosed are compounds, compositions and methods for treating disease, syndromes, conditions and disorders that are affected by the modulation of PKC-theta. Such compounds are represented by Formula I, wherein the variables are defined herein. (I)
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公开(公告)号：US20240197726A1
公开(公告)日：2024-06-20
申请号：US18280035
申请日：2022-03-01
发明人： Hiroki OGURI , Ryo TANIFUJI
IPC分类号： A61K31/4995 , A61P35/00 , C07D471/18 , C07D491/22 , C07D498/22
CPC分类号： A61K31/4995 , A61P35/00 , C07D471/18 , C07D491/22 , C07D498/22
摘要： [Problem] To provide: a novel tetrahydroisoquinoline (THIQ) alkaloid compound having a macrocyclic structure; an intermediate of the compound; and a method for producing the compound.
[Solution] Provided is a compound represented by formula (I), or a pharmaceutically acceptable salt thereof.
The present invention also provides: a method for synthesizing this compound; and an intermediate compound useful in this synthesis.-
公开(公告)号：US20240173317A1
公开(公告)日：2024-05-30
申请号：US18382636
申请日：2023-10-23
发明人： Thomas JAECKLIN
IPC分类号： A61K31/4995 , A61K9/00 , A61K9/08 , A61K31/07 , A61K31/355 , A61K31/593 , A61K47/10 , A61P1/16
CPC分类号： A61K31/4995 , A61K9/0053 , A61K9/08 , A61K31/07 , A61K31/355 , A61K31/593 , A61K47/10 , A61P1/16
摘要： Provided herein are methods for treating cholestasis in a subject having liver disease. More specifically, the present invention relates to methods for treating Progressive Familial Intrahepatic Cholestasis (PFIC) in a subject where the method includes administering maralixibat to a subject in need thereof.
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公开(公告)号：US20240139241A1
公开(公告)日：2024-05-02
申请号：US18492345
申请日：2023-10-23
IPC分类号： A61K35/15 , A61K31/4995 , A61K31/675 , A61K31/7076 , A61K39/00 , A61P35/00 , C07K16/28
CPC分类号： A61K35/15 , A61K31/4995 , A61K31/675 , A61K31/7076 , A61K39/4614 , A61K39/464429 , A61P35/00 , C07K16/2896 , A61K2239/15 , A61K2239/21 , A61K2239/22 , A61K2239/48
摘要： Compositions and methods for therapeutic use of engineered myeloid cells are described. Methods for increasing therapeutic effectiveness of immune cells by use of an immune cell inhibitory agent prior to therapy is described. Effective use of myeloid cells in combination therapy is described.
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公开(公告)号：US20240041873A1
公开(公告)日：2024-02-08
申请号：US18448122
申请日：2023-08-10
申请人： PHARMA MAR, S.A.
发明人： Carmen Kahatt , José María Fernandez , Salvador Fudio , Arturo Soto , Pilar Lardelli , Cristian Fernandez
IPC分类号： A61K31/4995 , A61P11/00 , A61P35/00 , A61K9/00 , A61K31/4738 , A61K31/4745 , A61K31/573 , A61K38/19 , C07D519/00
CPC分类号： A61K31/4995 , A61P11/00 , A61P35/00 , A61K9/0019 , A61K31/4738 , A61K31/4745 , A61K31/573 , A61K38/193 , C07D519/00 , C07B2200/13
摘要： Provided are methods for the treatment of SCLC patients by administering therapeutic amounts of lurbinectedin by intravenous infusion. Also provided are methods of treating cancer by administering lurbinectedin in combination with other anticancer drugs, in particular topoisomerase inhibitors. The invention further relates to the administration of lurbinectedin in combination with anti-emetic agents for effective control of symptoms related to nausea and vomiting, reduced lurbinectedin dosages to achieve a safer administration and an increase in the number of treatment cycles. Stable lyophilized formulations of lurbinectedin are also provided.
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公开(公告)号：US20230310426A1
公开(公告)日：2023-10-05
申请号：US18023804
申请日：2021-09-03
申请人： PHARMA MAR S.A.
发明人： Guido Kroemer , Oliver Kepp
IPC分类号： A61K31/4995 , A61P35/00 , A61K39/395
CPC分类号： A61K31/4995 , A61P35/00 , A61K39/3955 , A61K2039/505
摘要： Described are combination therapies for the treatment of solid tumours, said therapies comprising lurbinectedin and an immune checkpoint inhibitor, for example, anti-PD-1, anti-PD-L1 or anti-CTLA-4 antibodies.
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公开(公告)号：US20230279012A1
公开(公告)日：2023-09-07
申请号：US18069099
申请日：2022-12-20
申请人： Genentech, Inc.
IPC分类号： C07D487/04 , C07D487/14 , C07D471/04 , C07D471/14 , C07D495/04 , C07D519/00 , A61P37/00 , A61P35/00 , A61K31/496 , A61K31/4985 , A61K31/5025 , A61K31/506 , A61K31/53 , A61K31/5377 , A61K31/5383 , A61K45/06 , C07D495/14 , C07D498/04 , A61K31/4995 , A61K31/501 , C07D487/08 , C07D513/04 , A61K31/495 , A61K9/20
CPC分类号： C07D487/04 , C07D487/14 , C07D471/04 , C07D471/14 , C07D495/04 , C07D519/00 , A61P37/00 , A61P35/00 , A61K31/496 , A61K31/4985 , A61K31/5025 , A61K31/506 , A61K31/53 , A61K31/5377 , A61K31/5383 , A61K45/06 , C07D495/14 , C07D498/04 , A61K31/4995 , A61K31/501 , C07D487/08 , C07D513/04 , A61K31/495 , A61K9/20
摘要： Heteroaryl pyridone and aza-pyridone compounds are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using heteroaryl pyridone and aza-pyridone compounds for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
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公开(公告)号：US11730724B2
公开(公告)日：2023-08-22
申请号：US17082902
申请日：2020-10-28
申请人： Bow River LLC
发明人： Sundar Srinivasan , Christina Chow
IPC分类号： A61K31/4468 , A61K31/454 , A61K31/519 , A61K31/498 , A61K31/497 , A61K31/506 , A61K31/407 , A61P35/04 , A61K9/00 , A61K31/5383 , A61P25/18 , A61K31/4995 , A61P25/16 , A61K31/4745 , A61K31/397 , A61K31/5395 , A61P35/02 , A61K9/08 , A61K9/20 , A61K9/48 , A61K31/00 , A61K9/10
CPC分类号： A61K31/4468 , A61K9/0019 , A61K9/0053 , A61K9/0056 , A61K9/0078 , A61K9/0095 , A61K9/08 , A61K9/10 , A61K9/2004 , A61K9/4841 , A61K31/00 , A61K31/397 , A61K31/407 , A61K31/454 , A61K31/4745 , A61K31/497 , A61K31/498 , A61K31/4995 , A61K31/506 , A61K31/519 , A61K31/5383 , A61K31/5395 , A61P25/16 , A61P25/18 , A61P35/02 , A61P35/04
摘要： The present disclosure provides for methods of treating a patient with a CYP3A4 substrate drug, wherein the patient is treated with posaconazole. In some embodiments, the patient stops posaconazole treatment, waits for at least 2 days, and then is treated with the CYP3A4 substrate drug as soon as it is safe to do so. In some embodiments, treatment with the CYP3A4 substrate drug is delayed for about 2-42 days after stopping posaconazole. In some embodiments, the patient is treated with a reduced dose of the CYP3A4 substrate drug for about 2-42 days.
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