公开(公告)号：US20240308960A1

公开(公告)日：2024-09-19

申请号：US18563776

申请日：2022-05-26

Applicant: Sumitomo Pharma Co., Ltd.

Inventor： Masafumi KOMIYA ,  Shunichiro UESUGI ,  Eiji IDEUE ,  Shoukou LEE ,  Daisuke TANAKA ,  Yuta FUNAKOSHI

IPC: C07D211/22 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/5355 ,  A61K31/55 ,  A61K31/551 ,  C07D211/16 ,  C07D211/26 ,  C07D211/46 ,  C07D221/04 ,  C07D223/16 ,  C07D401/04 ,  C07D401/12 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04

CPC classification number: C07D211/22 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/5355 ,  A61K31/55 ,  A61K31/551 ,  C07D211/16 ,  C07D211/26 ,  C07D211/46 ,  C07D221/04 ,  C07D223/16 ,  C07D401/04 ,  C07D401/12 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04

Abstract: The present invention relates to a medicament for treating or preventing a disease related to orexin receptor, especially orexin receptor type 2, comprising a new compound having a urea structure or a pharmaceutically acceptable salt thereof as an active ingredient. In more detail, the present invention relates to a medicament for treating or preventing a disease such as narcolepsy, idiopathic hypersomnia, hypersomnia, sleep apnea syndrome.

公开(公告)号：US20240299438A1

公开(公告)日：2024-09-12

申请号：US18270915

申请日：2021-12-31

Applicant: DONGGUK UNIVERSITY INDUSTRY-ACADEMIC COOPERATION FOUNDATION

Inventor： Jongpil KIM ,  Hongwon KIM ,  Byounggook CHO

IPC: A61K31/7105 ,  A01K67/027 ,  A61K31/5355 ,  A61P25/18 ,  G01N33/50

CPC classification number: A61K31/7105 ,  A01K67/027 ,  A61K31/5355 ,  A61P25/18 ,  G01N33/5058 ,  G01N33/5073 ,  A01K2207/05 ,  A01K2207/20

Abstract: Provided are diagnosis and treatment methods of autism spectrum disorder, based on an activity regulation mechanism of quiescent neural stem cells, and use thereof.

公开(公告)号：US12054472B2

公开(公告)日：2024-08-06

申请号：US17239137

申请日：2021-04-23

Applicant: Nxera Pharma UK Limited

Inventor： Miles Stuart Congreve ,  Stephen Philippe Andrews ,  Jonathan Stephen Mason ,  Christine Mary Richardson ,  Giles Albert Brown

IPC: A61K31/506 ,  A61K31/4427 ,  A61K31/53 ,  A61K31/5355 ,  A61K31/5377 ,  A61K31/5386 ,  C07D253/07 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/04 ,  C07D405/10 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D487/04

CPC classification number: C07D401/04 ,  A61K31/4427 ,  A61K31/506 ,  A61K31/53 ,  A61K31/5355 ,  A61K31/5377 ,  A61K31/5386 ,  C07D253/07 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/04 ,  C07D405/10 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D487/04

Abstract: According to the invention there is provided a compound of formula A1 which may be useful in the treatment of a condition or disorder ameliorated by the inhibition of the A1-A2b or, particularly, the A2a receptor. A process for the preparation of the compound, pharmaceutical compositions comprising the compound, and methods of treatment comprising administration of an effective amount of the compound are also disclosed.

公开(公告)号：US20240217959A1

公开(公告)日：2024-07-04

申请号：US18554195

申请日：2022-04-06

Applicant: ACONDICIONAMIENTO TARRASENSE

Inventor： José Luis DÍAZ-FERNÁNDEZ ,  Carmen ALMANSA-ROSALES ,  Ute CHRISTMANN

IPC: C07D413/14 ,  A61K31/506 ,  A61K31/5355 ,  A61K31/551 ,  A61K31/553 ,  C07D401/14 ,  C07D491/107

CPC classification number: C07D413/14 ,  A61K31/506 ,  A61K31/5355 ,  A61K31/551 ,  A61K31/553 ,  C07D401/14 ,  C07D491/107

Abstract: The present invention relates to new compounds of formula (I) as sigma ligands having a great affinity for sigma receptors, sigma-1 receptor (σ1) and/or sigma-2 receptor (σ2). The present invention also refers to the process for the preparation thereof, to compositions comprising them, and to their use as medicaments.

公开(公告)号：US20240101671A1

公开(公告)日：2024-03-28

申请号：US18273725

申请日：2022-01-20

Applicant: Zelarion Malta Limited

Inventor： Erik BERGLUND

IPC: C07K16/28 ,  A61K31/436 ,  A61K31/5355 ,  A61K31/573 ,  A61K31/675 ,  A61K35/407 ,  A61K39/395 ,  A61P37/06

CPC classification number: C07K16/2806 ,  A61K31/436 ,  A61K31/5355 ,  A61K31/573 ,  A61K31/675 ,  A61K35/407 ,  A61K39/3955 ,  A61P37/06 ,  A61K2039/505 ,  C07K2317/24 ,  C07K2317/565

Abstract: Provided herein are methods for inducing tolerance to an organ (e.g., liver) transplant in a patient. Compositions for use with these methods and kits are also disclosed.

公开(公告)号：US11925690B2

公开(公告)日：2024-03-12

申请号：US17251615

申请日：2019-06-13

Applicant: AMPHISTA THERAPEUTICS LTD

Inventor： Alessio Ciulli ,  Andrea Testa ,  Scott Hughes ,  Steven Peter Butcher

IPC: A61K47/60 ,  A61K31/277 ,  A61K31/351 ,  A61K31/404 ,  A61K31/407 ,  A61K31/4184 ,  A61K31/423 ,  A61K31/428 ,  A61K31/4375 ,  A61K31/44 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5355 ,  A61K31/551 ,  A61K47/55 ,  C07D417/14 ,  C07D495/14

CPC classification number: A61K47/60 ,  A61K31/277 ,  A61K31/351 ,  A61K31/404 ,  A61K31/407 ,  A61K31/4184 ,  A61K31/423 ,  A61K31/428 ,  A61K31/4375 ,  A61K31/44 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5355 ,  A61K31/551 ,  A61K47/55 ,  C07D417/14 ,  C07D495/14

Abstract: The invention provides for bifunctional molecules comprising an Rpn11 binding partner and a target protein binding partner. A bifunctional molecule according to the invention binds to Rpn11 and to the target protein, thereby facilitating degradation of the target protein bound to the target protein binding partner. The invention also provides for use of a bifunctional molecule for preventing or treating disease.

公开(公告)号：US20240033330A1

公开(公告)日：2024-02-01

申请号：US18475323

申请日：2023-09-27

Applicant: St. Vincent's Institute of Medical Research

Inventor： Helen E. Thomas ,  Thomas W. H. Kay ,  Balasubramanian Krishnamurthy ,  Gaurang Jhala

IPC: A61K38/28 ,  A61P3/10 ,  A61K31/437 ,  A61K31/4985 ,  A61K31/519 ,  A61K31/529 ,  A61K31/5355 ,  A61K31/541 ,  A61K31/553 ,  A61K38/17 ,  A61K38/46 ,  A61K38/51

CPC classification number: A61K38/28 ,  A61P3/10 ,  A61K31/437 ,  A61K31/4985 ,  A61K31/519 ,  A61K31/529 ,  A61K31/5355 ,  A61K31/541 ,  A61K31/553 ,  A61K38/1709 ,  A61K38/465 ,  A61K38/51

Abstract: The present invention relates to novel methods and therapies for treating, preventing or delaying the onset of type 1 diabetes. In one aspect, the invention provides a method of preventing, delaying the onset of, or delaying the progression of, type 1 diabetes (T1D) in an individual, the method comprising providing in the individual an anti-inflammatory compound; and a pancreatic autoantigen or a derivative or variant thereof; thereby preventing, delaying the onset of, or delaying the progression of, T1D in the individual.

公开(公告)号：US11839613B2

公开(公告)日：2023-12-12

申请号：US16614209

申请日：2018-05-17

Applicant: IDORSIA PHARMACEUTICALS LTD

Inventor： Christoph Boss ,  Olivier Corminboeuf ,  Heinz Fretz ,  Isabelle Lyothier ,  Davide Pozzi ,  Sylvia Richard-Bildstein ,  Hervé Siendt ,  Thierry Sifferlen

IPC: A61K31/506 ,  A61K45/06 ,  C07D409/12 ,  C07D409/14 ,  C07D239/26 ,  A61K31/505 ,  C07D405/14 ,  C07D405/12 ,  C07D413/14 ,  C07D401/14 ,  A61K31/5355 ,  C07D417/14 ,  A61P35/00 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12

CPC classification number: A61K31/506 ,  A61K31/505 ,  A61K31/5355 ,  A61K45/06 ,  A61P35/00 ,  C07D239/26 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14

Abstract: The present invention relates to pyrimidine derivatives of formula (I)




wherein (R1)n, R3, R4a, R4b, R5a, R5b and Ar1 are as described in the description and their use in the treatment of cancer by modulating an immune response comprising a reactivation of the immune system in the tumor. The invention further relates to novel benzofurane and benzothiophene derivatives of formula (II) and their use as pharmaceuticals, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), and especially to their use as modulators of the prostaglandin 2 receptors EP2 and/or EP4.

公开(公告)号：US20230381144A1

公开(公告)日：2023-11-30

申请号：US18204983

申请日：2023-06-02

Applicant: SYNVENTA LLC

Inventor： Artour Gomtsian ,  Anton Bespalov

IPC: A61K31/4174 ,  A61P43/00 ,  A61P25/02 ,  A61K31/506 ,  A61K31/4178 ,  A61K31/416 ,  A61K31/5355 ,  A61K31/4725 ,  A61K31/517

CPC classification number: A61K31/4174 ,  A61P43/00 ,  A61P25/02 ,  A61K31/506 ,  A61K31/4178 ,  A61K31/416 ,  A61K31/5355 ,  A61K31/4725 ,  A61K31/517

Abstract: The present disclosure relates to compositions comprising a TRPV1 antagonist and an Alpha-2 adrenoceptor agonist useful in the treatment of various forms of pain, including chronic pain (CP) syndromes, inflammatory pain and pain associated with neuropathy and other diseases and disease states and methods of use thereof and methods of treatment of various forms of pain, including chronic pain (CP) syndromes, inflammatory pain and pain associated with neuropathy and other diseases and disease states, and methods of reducing a TRPV1 antagonist-induced increase in body temperature in a mammal, comprising administering a therapeutically effective amount of a pharmaceutical composition for comprising alpha-2 adrenoceptor agonist.

公开(公告)号：US11679113B2

公开(公告)日：2023-06-20

申请号：US16824639

申请日：2020-03-19

Applicant: The Regents of the University of California

Inventor： Jorge Gutkind ,  David Schlaepfer ,  Justine Paradis ,  Ayush Kishore ,  Monica Acosta ,  Nadia Arang

IPC: A61P35/04 ,  A61K31/506 ,  A61K31/5355 ,  A61K31/437 ,  A61K31/136 ,  A61K31/4402 ,  A61K31/166 ,  A61K31/4184 ,  A61K31/519 ,  A61K31/44 ,  A61K31/4523 ,  A61K31/53 ,  A61K31/4439 ,  A61K48/00 ,  A61K31/5025

CPC classification number: A61K31/5355 ,  A61K31/5025 ,  A61K48/005 ,  A61P35/04

Abstract: Provided herein are methods for treating uveal melanoma in a subject in need thereof by administering an effective amount of an agent that inhibits expression of FAK protein to the subject. In one aspect, the agent that inhibits expression of FAK protein comprises, or alternatively consists essentially of, or yet further consists of a gene editing agent, such as for example one or more of: RNA interference (RNAi), CRISPR/Cas, ZFN, and/or TALEN. In another aspect, the agent is VS-4718. Also described herein are kits comprising, or alternatively consisting essentially of, or yet further consisting of one or more of: agents that inhibit expression of FAK protein, siRNAs, shRNAs, miRNAs, nucleases and/or guide RNA sequences for carrying out the methods of this disclosure, and optional instructions for use.