公开(公告)号：US20240317763A1

公开(公告)日：2024-09-26

申请号：US18583627

申请日：2024-02-21

申请人： Infinity Pharmaceuticals, Inc.

发明人： Louis Grenier ,  Andre Lescarbeau ,  Praveen Sharma ,  Daniel G. Genov

IPC分类号： C07D487/04 ,  A61K9/48 ,  A61K31/519 ,  C07D231/12 ,  C07D231/38 ,  C07D401/06

CPC分类号： C07D487/04 ,  A61K9/485 ,  A61K9/4858 ,  A61K9/4866 ,  A61K31/519 ,  C07D231/12 ,  C07D231/38 ,  C07D401/06 ,  C07B2200/13

摘要： Solid forms of chemical compounds that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein. Also provided herein are processes for preparing compounds, polymorphic forms, cocrystals, and amorphous forms thereof, and pharmaceutical compositions thereof.

公开(公告)号：US20240293318A1

公开(公告)日：2024-09-05

申请号：US18440188

申请日：2024-02-13

申请人： Flagship Pioneering Innovations VII, LLC

发明人： Timothy Ray Blake ,  Dean Peter Stamos

IPC分类号： A61K9/127 ,  A61K9/51 ,  A61K45/06 ,  C07C211/03 ,  C07C307/06 ,  C07D231/38 ,  C07D241/08 ,  C07D241/20 ,  C07D249/14 ,  C07D251/10 ,  C07D265/32 ,  C07D285/10 ,  C07D285/16 ,  C07D305/12 ,  C07D307/33 ,  C07D309/30 ,  C07D319/12 ,  C07F9/24

CPC分类号： A61K9/1271 ,  A61K9/5123 ,  A61K45/06 ,  C07C211/03 ,  C07C307/06 ,  C07D231/38 ,  C07D241/08 ,  C07D241/20 ,  C07D249/14 ,  C07D251/10 ,  C07D265/32 ,  C07D285/10 ,  C07D285/16 ,  C07D305/12 ,  C07D307/33 ,  C07D309/30 ,  C07D319/12 ,  C07F9/2458

摘要： The present disclosure relates to a lipid compound of formula (Ia) or (AL-GI):




having various cleavable linkers defined by the variables Z1 and Z2 and Z10 and Z20. The present disclosure also relates to a lipid carrier or lipid nanoformulation employing the lipid compound, and the use of the lipid compound in a pharmaceutical composition as well as for a method of delivering an effector, e.g., a therapeutic agent.

公开(公告)号：US20240246950A1

公开(公告)日：2024-07-25

申请号：US18600161

申请日：2024-03-08

申请人： Ensem Therapeutics

发明人： Tao Liu

IPC分类号： C07D417/12 ,  A61P35/00 ,  C07D231/38 ,  C07D401/12 ,  C07D403/12 ,  C07D409/12 ,  C07D413/12 ,  C07D419/12 ,  C07D495/04

CPC分类号： C07D417/12 ,  A61P35/00 ,  C07D231/38 ,  C07D401/12 ,  C07D403/12 ,  C07D409/12 ,  C07D413/12 ,  C07D419/12 ,  C07D495/04

摘要： The invention provides novel anilino-pyrazole derivatives as a cyclin-dependent kinase 2 (CDK2) inhibitors. The invention also provides pharmaceutical compositions comprising the compounds and methods thereof for treating various conditions, diseases and disorders associated with or related to CDK2 activities, or associated with abnormal cell growth, such as tumor growth and cancer.

公开(公告)号：US20240246915A1

公开(公告)日：2024-07-25

申请号：US18423733

申请日：2024-01-26

申请人： Calgent Biotechnology Co., Ltd.

发明人： Yun YEN ,  Jing-ping LIOU ,  Shiow-lin PAN

IPC分类号： C07D213/75 ,  A61K31/166 ,  A61K31/167 ,  A61K31/4409 ,  A61K33/243 ,  A61P3/10 ,  A61P25/28 ,  A61P35/02 ,  A61P37/00 ,  C07D209/04 ,  C07D213/74 ,  C07D213/76 ,  C07D215/40 ,  C07D215/42 ,  C07D231/38 ,  C07D235/30 ,  C07D239/42 ,  C07D241/04 ,  C07D241/20 ,  C07D277/42 ,  C07D471/04 ,  C07D487/04 ,  A61K31/337 ,  A61K31/475 ,  A61K31/506 ,  A61K31/593 ,  A61K31/704 ,  A61K33/24

CPC分类号： C07D213/75 ,  A61K31/166 ,  A61K31/167 ,  A61K31/4409 ,  A61K33/243 ,  A61P3/10 ,  A61P25/28 ,  A61P35/02 ,  A61P37/00 ,  C07D209/04 ,  C07D213/74 ,  C07D213/76 ,  C07D215/40 ,  C07D215/42 ,  C07D231/38 ,  C07D235/30 ,  C07D239/42 ,  C07D241/04 ,  C07D241/20 ,  C07D277/42 ,  C07D471/04 ,  C07D487/04 ,  A61K31/337 ,  A61K31/475 ,  A61K31/506 ,  A61K31/593 ,  A61K31/704 ,  A61K33/24 ,  A61K2300/00

摘要： The invention relates to new compounds of formula (I)




with low cytotoxicity for blocking the ubiquitination-proteasome system in diseases. Accordingly, these compounds can be used in treatment of disorders including, but not limited to, cancers.

公开(公告)号：US12030869B2

公开(公告)日：2024-07-09

申请号：US17989237

申请日：2022-11-17

申请人： Assembly Biosciences, Inc.

发明人： Simon Nicolas Haydar ,  Leping Li ,  Mark G. Bures ,  Roopa Rai ,  Lynne Bannen ,  Michael Walker

IPC分类号： C07D231/38 ,  A61P31/20 ,  C07D401/08 ,  C07D403/04 ,  C07D403/08 ,  C07D403/10 ,  C07D403/12 ,  C07D405/04 ,  C07D413/04 ,  C07D413/08 ,  C07D417/08

CPC分类号： C07D403/08 ,  A61P31/20 ,  C07D231/38 ,  C07D401/08 ,  C07D403/04 ,  C07D403/10 ,  C07D403/12 ,  C07D405/04 ,  C07D413/04 ,  C07D413/08 ,  C07D417/08

摘要： The present disclosure provides, in part, 5-membered heteroaryl carboxamide compounds, and pharmaceutical compositions thereof, useful for disruption of HBV core protein assembly, and methods of treating Hepatitis B (HBV) infection.

公开(公告)号：US12012397B2

公开(公告)日：2024-06-18

申请号：US17967599

申请日：2022-10-17

申请人： NodThera Limited

发明人： David Harrison ,  Alan Paul Watt ,  Mark G. Bock

IPC分类号： C07D403/12 ,  C07D231/38 ,  C07D237/20 ,  C07D239/42 ,  C07D249/04 ,  C07D249/14 ,  C07D261/14 ,  C07D277/52 ,  C07D285/135 ,  C07D307/66 ,  C07D401/12 ,  C07D405/12 ,  C07D471/08

CPC分类号： C07D403/12 ,  C07D231/38 ,  C07D237/20 ,  C07D239/42 ,  C07D249/04 ,  C07D249/14 ,  C07D261/14 ,  C07D277/52 ,  C07D285/135 ,  C07D307/66 ,  C07D401/12 ,  C07D405/12 ,  C07D471/08 ,  C07B2200/05

摘要： The present disclosure relates to compounds of Formula (I):




and to their pharmaceutically acceptable salts, pharmaceutical compositions, methods of use, and methods for their preparation. The compounds disclosed herein are useful for inhibiting the maturation of cytokines of the IL-1 family by inhibiting inflammasomes and may be used in the treatment of disorders in which inflammasome activity is implicated, such as inflammatory, autoinflammatory and autoimmune diseases and cancers.

公开(公告)号：US20240182714A1

公开(公告)日：2024-06-06

申请号：US18435961

申请日：2024-02-07

申请人： The Government of the United States of America, as represented by the Secretary of the Navy

发明人： Brett D. Martin ,  Ian D. Giles ,  Jawad Naciri ,  Paul T. Charles ,  Scott A. Trammell ,  Jeffrey R. Deschamps ,  Jeffrey C. Depriest

IPC分类号： C08L79/04 ,  C07D231/38 ,  C08G73/06 ,  H01B1/12

CPC分类号： C08L79/04 ,  C07D231/38 ,  C08G73/0616 ,  C08L2203/204 ,  H01B1/127

摘要： This disclosure concerns electrically conducting poly(pyrazoles). The concept of oligomerizing and polymerizing substituted aminopyrazole derivatives combined with a monomer activation procedure involving base-mediated conversion of the protonated pyrazole ring nitrogen to amine salt was developed. This disclosure concerns the specific chemistries needed for the synthesis of a pyrazole monomer used in the polymer synthesis. The procedure used for blending the novel polypyrazoles with other compounds needed for construction of solar cells for testing was developed. This disclosure concerns the concept of using these types of heteroatom-rich, electron-deficient oligomers or polymers as n-dopable or p-dopable electron acceptors in photovoltaic cells. This disclosure concerns synthesizing the starting monomer compounds and polypyrazoles.

公开(公告)号：US11964968B2

公开(公告)日：2024-04-23

申请号：US18165037

申请日：2023-02-06

申请人： Eli Lilly and Company

发明人： Erin D. Anderson ,  Steven W. Andrews ,  Kevin R. Condroski ,  Thomas C. Irvin ,  Gabrielle R. Kolakowski ,  Manoj Kumar ,  Elizabeth A. McFaddin ,  Megan McKenney ,  Michael J. Munchhof ,  Michael B. Welch

IPC分类号： C07D413/14 ,  C07D231/38 ,  C07D413/12 ,  C07D417/12

CPC分类号： C07D413/14 ,  C07D231/38 ,  C07D413/12 ,  C07D417/12 ,  C07B2200/05

摘要： Provided herein are RET kinase inhibitors according to the formula:




pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof, and methods for their use in the treatment of diseases that can be treated with a RET kinase inhibitor, including RET-associated diseases and disorders. A, R1, n, X1, X2, X3, X4, and R2 have the meanings given in the specification.

公开(公告)号：US11963947B2

公开(公告)日：2024-04-23

申请号：US17058903

申请日：2019-05-28

申请人： HUA Medicine (Shanghai) Ltd.

发明人： Li Chen ,  Yongguo Li ,  Gaosen Wang ,  Huisheng Gao

IPC分类号： A61K31/4155 ,  A61K9/16 ,  A61K9/20 ,  A61K9/28 ,  A61K31/155 ,  A61K31/40 ,  A61K31/403 ,  A61K31/4035 ,  A61K31/4439 ,  A61K31/4985 ,  A61K31/522 ,  A61K31/7034 ,  A61K45/06 ,  A61K47/38 ,  A61P3/10 ,  C07D231/38 ,  C07D403/12

CPC分类号： A61K31/4155 ,  A61K9/1611 ,  A61K9/1617 ,  A61K9/1635 ,  A61K9/1694 ,  A61K9/2009 ,  A61K9/2013 ,  A61K9/2027 ,  A61K9/2054 ,  A61K9/2086 ,  A61K9/2095 ,  A61K9/2813 ,  A61K9/284 ,  A61K9/2866 ,  A61K31/155 ,  A61K31/40 ,  A61K31/403 ,  A61K31/4035 ,  A61K31/4439 ,  A61K31/4985 ,  A61K31/522 ,  A61K31/7034 ,  A61K45/06 ,  A61K47/38 ,  A61P3/10 ,  C07D231/38 ,  C07D403/12

摘要： Disclosed is a pharmaceutical combination comprising a glucokinase activator or a pharmaceutically acceptable salt thereof, an isotopic label thereof, a crystalline form thereof, a hydrate, a solvate, a diastereomeric or enantiomeric form thereof, and a DPP-IV inhibitor. Disclosed are a pharmaceutical composition and a fixed dose of a compound preparation, and the methods for preparing the pharmaceutical composition and the fixed dose of the compound preparation and the uses thereof.

公开(公告)号：US11939333B2

公开(公告)日：2024-03-26

申请号：US17578309

申请日：2022-01-18

申请人： Infinity Pharmaceuticals, Inc.

发明人： Louis Grenier ,  Andre Lescarbeau ,  Praveen Sharma ,  Daniel G. Genov

IPC分类号： C07D487/04 ,  A61K9/48 ,  A61K31/519 ,  C07D231/12 ,  C07D231/38 ,  C07D401/06

CPC分类号： C07D487/04 ,  A61K9/485 ,  A61K9/4858 ,  A61K9/4866 ,  A61K31/519 ,  C07D231/12 ,  C07D231/38 ,  C07D401/06 ,  C07B2200/13

摘要： Solid forms of chemical compounds that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein. Also provided herein are processes for preparing compounds, polymorphic forms, cocrystals, and amorphous forms thereof, and pharmaceutical compositions thereof.