公开(公告)号：US20240358688A1

公开(公告)日：2024-10-31

申请号：US18756533

申请日：2024-06-27

Applicant: Boehringer Ingelheim International GmbH

Inventor： Harald ENGELHARDT ,  Mark PETRONCZKI ,  Juergen RAMHARTER ,  Ulrich REISER ,  Heinz STADTMUELLER ,  Dirk SCHARN ,  Tobias WUNBERG

IPC: A61K31/437 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/4995 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/541 ,  A61K31/553 ,  A61P35/00 ,  C07D211/04 ,  C07D519/00

CPC classification number: A61K31/437 ,  A61K31/4545 ,  A61K31/4995 ,  A61K31/553 ,  A61P35/00 ,  C07D211/04 ,  C07D519/00 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/541

Abstract: 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：US12064421B2

公开(公告)日：2024-08-20

申请号：US17514145

申请日：2021-10-29

Applicant: Boehringer Ingelheim International GmbH

Inventor： Harald Engelhardt ,  Mark Petronczki ,  Juergen Ramharter ,  Ulrich Reiser ,  Heinz Stadtmueller ,  Dirk Scharn ,  Tobias Wunberg

IPC: C07D211/04 ,  A61K31/437 ,  A61K31/4545 ,  A61K31/4995 ,  A61K31/553 ,  A61P35/00 ,  C07D519/00 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/541

CPC classification number: A61K31/437 ,  A61K31/4545 ,  A61K31/4995 ,  A61K31/553 ,  A61P35/00 ,  C07D211/04 ,  C07D519/00 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/541

Abstract: 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

Applicant: Exscientia Al Limited

Inventor： Peter Ray ,  Anthony Bradley ,  Simon Richards ,  Catarina Santos ,  Jeremy Besnard ,  Jérôme Meneyrol ,  Virginie Suchaud

IPC: 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 classification number: 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

Abstract: 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)

公开(公告)号：US20240197726A1

公开(公告)日：2024-06-20

申请号：US18280035

申请日：2022-03-01

Applicant: THE UNIVERSITY OF TOKYO

Inventor： Hiroki OGURI ,  Ryo TANIFUJI

IPC: A61K31/4995 ,  A61P35/00 ,  C07D471/18 ,  C07D491/22 ,  C07D498/22

CPC classification number: A61K31/4995 ,  A61P35/00 ,  C07D471/18 ,  C07D491/22 ,  C07D498/22

Abstract: [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

Applicant: MIRUM PHARMACEUTICALS, INC.

Inventor： Thomas JAECKLIN

IPC: A61K31/4995 ,  A61K9/00 ,  A61K9/08 ,  A61K31/07 ,  A61K31/355 ,  A61K31/593 ,  A61K47/10 ,  A61P1/16

CPC classification number: A61K31/4995 ,  A61K9/0053 ,  A61K9/08 ,  A61K31/07 ,  A61K31/355 ,  A61K31/593 ,  A61K47/10 ,  A61P1/16

Abstract: 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.

公开(公告)号：US20240139241A1

公开(公告)日：2024-05-02

申请号：US18492345

申请日：2023-10-23

Applicant: Myeloid Therapeutics, Inc.

Inventor： Daniel GETTS ,  Bruce J. McCreedy, JR. ,  Michele Luise Gerber ,  Thomas Etienne Prod’homme

IPC: A61K35/15 ,  A61K31/4995 ,  A61K31/675 ,  A61K31/7076 ,  A61K39/00 ,  A61P35/00 ,  C07K16/28

CPC classification number: A61K35/15 ,  A61K31/4995 ,  A61K31/675 ,  A61K31/7076 ,  A61K39/4614 ,  A61K39/464429 ,  A61P35/00 ,  C07K16/2896 ,  A61K2239/15 ,  A61K2239/21 ,  A61K2239/22 ,  A61K2239/48

Abstract: 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.

公开(公告)号：US20240041873A1

公开(公告)日：2024-02-08

申请号：US18448122

申请日：2023-08-10

Applicant: PHARMA MAR, S.A.

Inventor： Carmen Kahatt ,  José María Fernandez ,  Salvador Fudio ,  Arturo Soto ,  Pilar Lardelli ,  Cristian Fernandez

IPC: A61K31/4995 ,  A61P11/00 ,  A61P35/00 ,  A61K9/00 ,  A61K31/4738 ,  A61K31/4745 ,  A61K31/573 ,  A61K38/19 ,  C07D519/00

CPC classification number: A61K31/4995 ,  A61P11/00 ,  A61P35/00 ,  A61K9/0019 ,  A61K31/4738 ,  A61K31/4745 ,  A61K31/573 ,  A61K38/193 ,  C07D519/00 ,  C07B2200/13

Abstract: 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.

公开(公告)号：US20230310426A1

公开(公告)日：2023-10-05

申请号：US18023804

申请日：2021-09-03

Applicant: PHARMA MAR S.A.

Inventor： Guido Kroemer ,  Oliver Kepp

IPC: A61K31/4995 ,  A61P35/00 ,  A61K39/395

CPC classification number: A61K31/4995 ,  A61P35/00 ,  A61K39/3955 ,  A61K2039/505

Abstract: 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.

公开(公告)号：US20230279012A1

公开(公告)日：2023-09-07

申请号：US18069099

申请日：2022-12-20

Applicant: Genentech, Inc.

Inventor： James John CRAWFORD ,  Daniel Fred ORTWINE ,  BinQing WEI ,  Wendy B. YOUNG

IPC: 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 classification number: 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

Abstract: 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.

公开(公告)号：US11730724B2

公开(公告)日：2023-08-22

申请号：US17082902

申请日：2020-10-28

Applicant: Bow River LLC

Inventor： Sundar Srinivasan ,  Christina Chow

IPC: 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 classification number: 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

Abstract: 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.