公开(公告)号：US12115157B2

公开(公告)日：2024-10-15

申请号：US17941860

申请日：2022-09-09

申请人： Boehringer Ingelheim International GmbH ,  Arena Pharmaceuticals, Inc.

发明人： Kai Gerlach ,  Daniela Gavina Berta ,  Marco Ferrara ,  Kirsten Gutsche ,  Ursula Mueller-Vieira ,  Scott Hobson ,  Frank Runge ,  Graeme Semple ,  Viktor Vintonyak ,  Yifeng Xiong

IPC分类号： A61K31/497 ,  A61K31/433 ,  A61K45/06 ,  C07D403/14 ,  C07D417/14 ,  C07D487/08

CPC分类号： A61K31/497 ,  A61K31/433 ,  A61K45/06 ,  C07D403/14 ,  C07D417/14 ,  C07D487/08 ,  C07B2200/05 ,  C07B2200/09

摘要： The invention relates to 3-phenoxyazetidin-1-yl-heteroaryl pyrrolidine derivatives of general formula (I) which are agonists of GPR52, useful in treating central nervous system diseases and other diseases.
In addition, the invention relates to the 3-phenoxyazetidin-1-yl-heteroaryl pyrrolidine derivatives of general formula (I) for use as a medicament, pharmaceutical compositions comprising at least a compound of general formula (I) and processes for preparing pharmaceutical compositions as well as processes for manufacture the compounds according to the invention.

公开(公告)号：US12109201B2

公开(公告)日：2024-10-08

申请号：US17843028

申请日：2022-06-17

申请人： Ovid Therapeutics, Inc.

发明人： Matthew During

IPC分类号： A61K31/437 ,  A61K9/00 ,  A61K31/165 ,  A61K31/19 ,  A61K31/195 ,  A61K31/197 ,  A61K31/27 ,  A61K31/325 ,  A61K31/36 ,  A61K31/4015 ,  A61K31/4166 ,  A61K31/4192 ,  A61K31/423 ,  A61K31/433 ,  A61K31/44 ,  A61K31/444 ,  A61K31/4535 ,  A61K31/513 ,  A61K31/515 ,  A61K31/53 ,  A61K31/55 ,  A61K31/5513 ,  A61K31/5517 ,  A61K31/57 ,  A61K31/7048 ,  A61K45/06

CPC分类号： A61K31/437 ,  A61K9/0019 ,  A61K31/165 ,  A61K31/19 ,  A61K31/195 ,  A61K31/197 ,  A61K31/27 ,  A61K31/325 ,  A61K31/36 ,  A61K31/4015 ,  A61K31/4166 ,  A61K31/4192 ,  A61K31/423 ,  A61K31/433 ,  A61K31/44 ,  A61K31/444 ,  A61K31/4535 ,  A61K31/513 ,  A61K31/515 ,  A61K31/53 ,  A61K31/55 ,  A61K31/5513 ,  A61K31/5517 ,  A61K31/57 ,  A61K31/7048 ,  A61K45/06 ,  A61K31/437 ,  A61K2300/00 ,  A61K31/57 ,  A61K2300/00 ,  A61K31/5517 ,  A61K2300/00 ,  A61K31/5513 ,  A61K2300/00 ,  A61K31/44 ,  A61K31/04 ,  A61K2300/00 ,  A61K2300/00 ,  A61K31/27 ,  A61K2300/00 ,  A61K31/433 ,  A61K2300/00 ,  A61K31/55 ,  A61K2300/00 ,  A61K31/4015 ,  A61K2300/00 ,  A61K31/195 ,  A61K2300/00 ,  A61K31/165 ,  A61K2300/00 ,  A61K31/53 ,  A61K2300/00 ,  A61K31/444 ,  A61K2300/00 ,  A61K31/515 ,  A61K2300/00 ,  A61K31/4166 ,  A61K2300/00 ,  A61K31/4192 ,  A61K2300/00 ,  A61K31/19 ,  A61K2300/00 ,  A61K31/513 ,  A61K2300/00 ,  A61K31/36 ,  A61K2300/00 ,  A61K31/4535 ,  A61K2300/00 ,  A61K31/7048 ,  A61K2300/00 ,  A61K31/197 ,  A61K2300/00 ,  A61K31/423 ,  A61K2300/00 ,  A61K31/136 ,  A61K2300/00

摘要： Use of allosteric modulators and/or gaboxadol for the treatment of epileptic disorders in a subject in need thereof.

公开(公告)号：US20240325354A1

公开(公告)日：2024-10-03

申请号：US18735806

申请日：2024-06-06

申请人： Alzheon, Inc.

发明人： Petr Kocis ,  Martin Tolar ,  John Hey

IPC分类号： A61K31/4196 ,  A61K31/426 ,  A61K31/433 ,  A61K31/44 ,  A61K31/505 ,  A61P25/28

CPC分类号： A61K31/4196 ,  A61K31/426 ,  A61K31/433 ,  A61K31/44 ,  A61K31/505 ,  A61P25/28

摘要： Methods of treating a disease characterized by amyloid aggregates are provided herein.

公开(公告)号：US20240277658A1

公开(公告)日：2024-08-22

申请号：US18030875

申请日：2021-10-15

申请人： ALBERT-LUDWIGS-UNIVERSITÄT FREIBURG

发明人： Olaf GROSS ,  Emilia NEUWIRT ,  Manfred JUNG

IPC分类号： A61K31/397 ,  A61K31/17 ,  A61K31/277 ,  A61K31/341 ,  A61K31/351 ,  A61K31/402 ,  A61K31/404 ,  A61K31/4178 ,  A61K31/421 ,  A61K31/4245 ,  A61K31/433 ,  A61K31/4375 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/5375 ,  A61P37/04

CPC分类号： A61K31/397 ,  A61K31/17 ,  A61K31/277 ,  A61K31/341 ,  A61K31/351 ,  A61K31/402 ,  A61K31/404 ,  A61K31/4178 ,  A61K31/421 ,  A61K31/4245 ,  A61K31/433 ,  A61K31/4375 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/5375 ,  A61P37/04

摘要： The present invention relates to a compound or pharmaceutically acceptable salts thereof, that modulates NLRP3 in that the NLRP3 inflammasome is activated. This invention further relates to the compounds and/or compositions for use in the prevention and treatment of a condition, disease or a disorder by activating the NLRP3 inflammasome, wherein the disease is selected from a group comprising infectious diseases, or cancer. Moreover, the invention relates to the use of the present compounds for analyzing a the activity of NLRP3 activation.

公开(公告)号：US20240262801A1

公开(公告)日：2024-08-08

申请号：US18534527

申请日：2023-12-08

申请人： Ness Therapeutics, Inc.

发明人： Volodymyr Kysil ,  Vladislav Zenonovich Parchinsky ,  Alexei Pushechnikov ,  Alexandre Vasilievich Ivachtchenko ,  Nikolay Savchuk

IPC分类号： C07D285/10 ,  A61K31/433 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/5377 ,  C07D417/12

CPC分类号： C07D285/10 ,  A61K31/433 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/5377 ,  C07D417/12

摘要： The present invention is generally directed to inhibitors of protein tyrosine phosphatase enzymes useful in the treatment of diseases and disorders modulated by said enzymes and having the Formula (I):

公开(公告)号：US20240238258A1

公开(公告)日：2024-07-18

申请号：US18389887

申请日：2023-12-20

申请人： BRISTOL-MYERS SQUIBB COMPANY

发明人： HAIBO LIU ,  YUCHENG MU ,  ANNAPURNA PENDRI ,  SHOSHANA L. POSY ,  JOANNE JEWETT BRONSON ,  LOUIS S. CHUPAK ,  LAURA AKULLIAN D'AGOSTINO

IPC分类号： A61K31/433 ,  A61K39/395 ,  C07D417/12

CPC分类号： A61K31/433 ,  A61K39/3955 ,  C07D417/12

摘要： Disclosed are compounds of Formula (I)




pharmaceutically acceptable salts thereof are defined herein, and pharmaceutical compositions thereof and combinations thereof, and methods of using the same as inhibitors of protein tyrosine phosphatases (PTPN2). These compounds are useful in treating cancer and diseases susceptible to PTPN2 inhibition.

公开(公告)号：US12023348B2

公开(公告)日：2024-07-02

申请号：US15569407

申请日：2016-04-26

申请人： The Medical Research, Infrastructure and Health Services Fund of the Tel Aviv Medical Center

发明人： Ofer Sarig ,  Eli Sprecher

IPC分类号： A61K31/704 ,  A61K31/122 ,  A61K31/137 ,  A61K31/167 ,  A61K31/277 ,  A61K31/365 ,  A61K31/366 ,  A61K31/37 ,  A61K31/404 ,  A61K31/423 ,  A61K31/427 ,  A61K31/433 ,  A61K31/4402 ,  A61K31/4453 ,  A61K31/4535 ,  A61K31/454 ,  A61K31/4738 ,  A61K31/4741 ,  A61K31/4745 ,  A61K31/475 ,  A61K31/498 ,  A61K31/53 ,  A61K31/538 ,  A61K31/5415 ,  A61K31/566 ,  A61K31/58 ,  A61K31/688 ,  A61K45/06 ,  A61P17/00 ,  A61P17/06

CPC分类号： A61K31/704 ,  A61K31/122 ,  A61K31/137 ,  A61K31/167 ,  A61K31/277 ,  A61K31/365 ,  A61K31/366 ,  A61K31/37 ,  A61K31/404 ,  A61K31/423 ,  A61K31/427 ,  A61K31/433 ,  A61K31/4402 ,  A61K31/4453 ,  A61K31/4535 ,  A61K31/454 ,  A61K31/4738 ,  A61K31/4741 ,  A61K31/4745 ,  A61K31/475 ,  A61K31/498 ,  A61K31/53 ,  A61K31/538 ,  A61K31/5415 ,  A61K31/566 ,  A61K31/58 ,  A61K31/688 ,  A61K45/06 ,  A61P17/00 ,  A61P17/06

摘要： A method of treating an inflammation or a hyperproliferative disease in a subject in need thereof is disclosed. The method comprising administering to the subject a therapeutically effective amount of a compound selected from the group consisting of:



a compound represented by Formula I:








or a pharmaceutically acceptable salt thereof,



a compound represented by Formula II:










and a compound represented by Formula III:








wherein the variables in Formulae I, II and III are as defined in the specification.

公开(公告)号：US20240165070A1

公开(公告)日：2024-05-23

申请号：US18461724

申请日：2023-09-06

申请人： Board of Regents, The University of Texas System

发明人： Timothy HEFFERNAN ,  Jeffrey KOVACS ,  Nakia SPENCER ,  Christopher BRISTOW

IPC分类号： A61K31/282 ,  A61K31/337 ,  A61K31/4196 ,  A61K31/433 ,  A61K31/501 ,  A61K31/55 ,  A61K33/243 ,  A61K45/06 ,  A61P35/00 ,  G01N33/574 ,  A61K51/04

CPC分类号： A61K31/282 ,  A61K31/337 ,  A61K31/4196 ,  A61K31/433 ,  A61K31/501 ,  A61K31/55 ,  A61K33/243 ,  A61K45/06 ,  A61P35/00 ,  G01N33/57449 ,  A61K51/0408

摘要： Disclosed herein are methods of treating a tumor or cancer in a subject whose tumor or cancer cells express low levels of asparagine synthetase (ASNS), and compounds and compositions useful in such treatment. Also disclosed herein are methods of evaluating whether to administer a compound that inhibits glutathione production or a glutaminase inhibitor to a subject with a tumor or cancer.

公开(公告)号：US11980607B2

公开(公告)日：2024-05-14

申请号：US18052369

申请日：2022-11-03

申请人： Actuate Therapeutics Inc.

发明人： Francis Giles ,  Andrew Mazar

IPC分类号： A61K31/407 ,  A61K31/433 ,  A61K31/52 ,  A61K31/5377 ,  A61K31/5517 ,  A61K31/635 ,  A61P35/02

CPC分类号： A61K31/407 ,  A61K31/433 ,  A61K31/52 ,  A61K31/5377 ,  A61K31/5517 ,  A61K31/635 ,  A61P35/02

摘要： Methods of treating malignant lymphoproliferative disorders in a patient, comprising administering an effective amount of a GSK-3β inhibitor, for example 9-ING-41, are provided. Also provided are methods for treating malignant lymphoproliferative disorders comprising administering a GSK-3β inhibitor, for example 9-ING-41, in combination with a second or multiple therapeutic agents.

公开(公告)号：US20240130983A1

公开(公告)日：2024-04-25

申请号：US18393798

申请日：2023-12-22

申请人： NLC Pharma Ltd

发明人： Dorit ARAD

IPC分类号： A61K31/122 ,  A61K9/00 ,  A61K9/127 ,  A61K9/20 ,  A61K9/28 ,  A61K9/48 ,  A61K31/198 ,  A61K31/222 ,  A61K31/381 ,  A61K31/40 ,  A61K31/422 ,  A61K31/433 ,  A61K31/454 ,  A61K31/513 ,  A61K31/536 ,  A61K36/30 ,  A61P31/14

CPC分类号： A61K31/122 ,  A61K9/0053 ,  A61K9/0095 ,  A61K9/127 ,  A61K9/2009 ,  A61K9/2013 ,  A61K9/2018 ,  A61K9/2054 ,  A61K9/2095 ,  A61K9/282 ,  A61K9/2833 ,  A61K9/4833 ,  A61K9/4858 ,  A61K9/4866 ,  A61K31/198 ,  A61K31/222 ,  A61K31/381 ,  A61K31/40 ,  A61K31/422 ,  A61K31/433 ,  A61K31/454 ,  A61K31/513 ,  A61K31/536 ,  A61K36/30 ,  A61P31/14 ,  A61K2236/51

摘要： Described herein are compounds of Formula I:




wherein R1-R6 are as described herein, for use in the treatment of a coronavirus infection; a method of inhibiting a coronavirus 3CL protease, by contacting the 3CL protease with a compound of Formula I; as well as methods pharmaceutical composition comprising a compound of Formula I and at least one phospholipid, wherein a weight ratio of the phospholipid(s) to the compound in the composition is in a range of from 10:1 to 1:10. Further described herein is a method of treating a coronavirus infection in a subject in need thereof, by administering to the subject at least one compound that exhibits at least two of: inhibition of an activity of a 3CL protease of the coronavirus; inhibition of inflammation in the subject; and inhibition of autophagy in the subject.