公开(公告)号：US20230039309A1

公开(公告)日：2023-02-09

申请号：US17518732

申请日：2021-11-04

申请人： Vanderbilt University

发明人： Taekyu Lee ,  Zhiguo Bian ,  Johannes Belmar ,  Plamen P. Christov ,  Nicholas F. Pelz ,  Subrata Shaw ,  Kwangho Kim ,  James C. Tarr ,  Edward T. Olejniczak ,  Bin Zhao ,  Stephen W. Fesik

IPC分类号： C07D487/04 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/14 ,  C07D209/42 ,  A61K31/551 ,  A61K31/381 ,  A61K31/4045 ,  A61K31/498 ,  C07D409/14 ,  C07D471/04 ,  C07D409/12 ,  A61K31/404 ,  A61K31/4155 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/5377 ,  A61K45/06 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14

摘要： The present invention provides for compounds that inhibit the activity of an anti-apoptotic Bcl-2 family member Myeloid cell leukemia-1 (Mcl-1) protein. The present invention also provides for pharmaceutical compositions as well as methods for using compounds for treatment of diseases and conditions (e.g., cancer) characterized by the over-expression or dysregulation of Mcl-1 protein.

公开(公告)号：US11559487B2

公开(公告)日：2023-01-24

申请号：US16707833

申请日：2019-12-09

申请人： SUN PHARMA ADVANCED RESEARCH COMPANY LIMITED

发明人： Ajay Jaysingh Khopade ,  Arindam Halder ,  Shivam Umeshkumar Upadhyay

IPC分类号： A61K9/14 ,  A61K9/00 ,  A61K9/20 ,  A61K9/10 ,  A61K9/06 ,  A61K31/135 ,  A61K31/196 ,  A61K31/335 ,  A61K31/498 ,  A61K31/519 ,  A61K31/65 ,  B82Y5/00 ,  A61K47/38 ,  A61K47/32

摘要： The present invention relates to nano-resin particles that are suitable for pharmaceutical use and their use in the pharmaceutical field. The present invention provides nano-sized resin particles having a particle size distribution characterized in that D90 value is between 200 nanometers to 900 nanometer and D10 value is not less than 50 nanometers, wherein the nano-resin particles are in pure form and safe for pharmaceutical use. The present invention further relates to pharmaceutical compositions comprising these purified nano-resin particles and their use in the treatment of diseases.
The present invention further provides a process for preparing purified, nano-sized resin particles that are suitable for pharmaceutical use, the process comprising steps of: (i) washing an ion exchange resin and suspending in an aqueous liquid, (ii) subjecting the suspension of (i) to wet milling for a period such that the particles have a particle size distribution characterized in that the D90 value is between 200 nanometers to 900 nanometers and D10 value is not less than 50 nanometers, (iii) subjecting the suspension of (ii) to purification to remove impurities, (iv) drying the purified suspension to obtain nano-resin particles in the form of dry powder.

公开(公告)号：US20230014173A1

公开(公告)日：2023-01-19

申请号：US17477970

申请日：2021-09-17

申请人： Janssen Sciences Ireland UC

发明人： Jérôme Émile Georges Guillemont ,  Magali Madeleine Simone Motte ,  Pierre Jean-Marie Bernard Rabiosson ,  Abdellah Tahri

IPC分类号： C07D401/12 ,  C07D403/12 ,  C07D401/14 ,  C07D487/04 ,  C07D487/10 ,  C07D513/04 ,  C07D519/00 ,  A61K45/06 ,  A61K31/404 ,  A61K31/429 ,  A61K31/437 ,  A61K31/438 ,  A61K31/444 ,  A61K31/4745 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/519 ,  C07D471/04 ,  A61P31/04 ,  A61K31/4709 ,  A61K31/498 ,  A61P31/06

摘要： The present invention relates to the following compounds wherein the integers are as defined in the description, and where the compounds may be useful as medicaments, for instance for use in the treatment of tuberculosis.

公开(公告)号：US11548901B2

公开(公告)日：2023-01-10

申请号：US16868119

申请日：2020-05-06

申请人： Gilead Sciences, Inc.

发明人： Elizabeth M. Bacon ,  Zhenhong R. Cai ,  Xiaowu Chen ,  Jeromy J. Cottell ,  Manoj C. Desai ,  Mingzhe Ji ,  Haolun Jin ,  Scott E. Lazerwith ,  Michael R. Mish ,  Philip Anthony Morganelli ,  Hyung-Jung Pyun ,  James G. Taylor ,  Teresa Alejandra Trejo Martin

IPC分类号： A61K31/4985 ,  C07D487/14 ,  C07D498/14 ,  A61K31/537 ,  C07D471/22 ,  A61K31/529 ,  A61K31/551 ,  A61K31/498 ,  C07D471/18 ,  A61K45/06 ,  C07D498/18 ,  A61K31/553

摘要： Compounds for use in the treatment of human immunodeficiency virus (HIV) infection are disclosed. The compounds have the following Formula (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein R1, X, W, Y1, Y2, Z1, and Z4 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

公开(公告)号：US20220409430A1

公开(公告)日：2022-12-29

申请号：US17902652

申请日：2022-09-02

申请人： TearClear Corp.

发明人： Michael T. MALANGA ,  Michael WILLIAMS ,  Srini VENKATESH

IPC分类号： A61F9/00 ,  A61K31/222 ,  B01J20/26 ,  B01J20/28 ,  A61K47/18 ,  A61K31/498

摘要： A system comprising a preservative-removing polymeric matrix comprising an active matrix component and an inactive matrix component. A method for administering an ophthalmic agent comprises providing a solution, emulsion, or suspension comprising an ophthalmic agent, and a preservative; and providing a preservative-removing polymeric matrix comprising an active matrix component and an inactive matrix component, and wherein the polymeric matrix is configured to selectively absorb the preservative when the solution, emulsion, or suspension is passed therethrough.

公开(公告)号：US20220395496A1

公开(公告)日：2022-12-15

申请号：US17761150

申请日：2020-09-14

申请人： Hoffmann-La Roche Inc.

发明人： Taishan HU ,  Buyu KOU ,  Haixia LIU ,  Hong SHEN ,  Wei ZHU ,  Ge ZOU

IPC分类号： A61K31/4709 ,  A61K31/498 ,  A61K31/4162 ,  A61K31/428

摘要： The present invention relates to compounds of formula (I), wherein R1, R2, R3, R4 and R5 are as described herein, and their pharmaceutically acceptable salt, enantiomer or diastereomer thereof, and compositions including the compounds and methods of using the compounds.

公开(公告)号：US20220370444A1

公开(公告)日：2022-11-24

申请号：US17755425

申请日：2020-11-01

申请人： MannKind Corporation

发明人： Thomas Hofmann ,  Stefan Ufer ,  Kevin Stapleton

IPC分类号： A61K31/498 ,  A61K9/00 ,  A61K9/16 ,  A61K31/47 ,  A61K31/606 ,  A61K31/546 ,  A61K31/7036 ,  A61K31/7048 ,  A61K31/4965 ,  A61K31/496 ,  A61K31/4709 ,  A61K31/5383

摘要： The present invention relates to pharmaceutical compositions for inhalation comprising a therapeutically effective dose of clofazimine wherein the clofazimine is provided in the form of dry powder, and processes for their preparation. Furthermore, the present invention provides pharmaceutical combinations comprising clofazimine in the form of an aerosol for pulmonary inhalation. The combinations and compositions provided by the present invention may be used in the treatment and/or prophylaxis of pulmonary infections caused by mycobacteria and other gram-positive bacteria, and of pulmonary fungal infections.

公开(公告)号：US20220348662A1

公开(公告)日：2022-11-03

申请号：US17763251

申请日：2020-09-25

申请人： JANSSEN PHARMACEUTICA NV

发明人： Waleed S. SHALABY ,  Ademi Elena SANTIAGO-WALKER ,  Raluca VERONA ,  Enrique ZUDAIRE

IPC分类号： C07K16/28 ,  A61K31/498 ,  A61K39/395 ,  A61P35/04 ,  A61P13/02

摘要： Embodiments of the present invention relate to a method of treating cancer in a patient comprising administering an immune checkpoint inhibitor to the patient, wherein the patient has been diagnosed with an FGFR-genetically altered cancer, and has been pre-treated with an FGFR inhibitor, such as erdafitinib.

公开(公告)号：US20220347173A1

公开(公告)日：2022-11-03

申请号：US17255168

申请日：2019-06-27

申请人： Blade Therapeutics, Inc.

发明人： Sharlene Lim ,  Prabha Ibrahim ,  Maria Fuentes

IPC分类号： A61K31/498 ,  A61K31/421 ,  A61K31/433 ,  A61K31/4439 ,  A61K31/166 ,  A61K31/415 ,  A61P1/16 ,  A61K45/06

摘要： Disclosed herein are methods of treating liver fibrosis by administering calpain inhibitors to subjects in need thereof.

公开(公告)号：US11478378B2

公开(公告)日：2022-10-25

申请号：US17394023

申请日：2021-08-04

申请人： TearClear Corp.

发明人： Michael T. Malanga ,  Michael Williams ,  Srini Venkatesh

IPC分类号： A61F9/00 ,  A61K31/222 ,  A61K31/498 ,  B01J20/28 ,  B01J20/26 ,  A61K47/18

摘要： A system comprising a preservative-removing polymeric matrix comprising an active matrix component and an inactive matrix component. A method for administering an ophthalmic agent comprises providing a solution, emulsion, or suspension comprising an ophthalmic agent, and a preservative; and providing a preservative-removing polymeric matrix comprising an active matrix component and an inactive matrix component, and wherein the polymeric matrix is configured to selectively absorb the preservative when the solution, emulsion, or suspension is passed therethrough.