公开(公告)号：US20240254077A1

公开(公告)日：2024-08-01

申请号：US18596300

申请日：2024-03-05

申请人： The Trustees of Columbia University in the City of New York

发明人： Jeanine D'Armiento

IPC分类号： C07C275/10 ,  A61K31/17 ,  A61K31/18 ,  C07C311/04 ,  C07C311/17

CPC分类号： C07C275/10 ,  A61K31/17 ,  A61K31/18 ,  C07C311/04 ,  C07C311/17

摘要： The present invention relates to the treatment of chronic obstructive pulmonary disease (COPD). More specifically, embodiments of the invention provide a pharmaceutical carrier and a compound that inhibit the induction of MMP-1 expression by cigarette smoke.

公开(公告)号：US20240174603A1

公开(公告)日：2024-05-30

申请号：US18273458

申请日：2022-02-07

申请人： Rappta Therapeutics Oy

发明人： George L. Trainor ,  Maria Obdulia Rabal Gracia ,  Laura Fourmois ,  Olga Gherbovet ,  Frederic Cachoux

IPC分类号： C07C311/18 ,  C07C311/17 ,  C07C311/19

CPC分类号： C07C311/18 ,  C07C311/17 ,  C07C311/19 ,  C07B2200/07

摘要： The present disclosure relates in part to chemical modulators of protein phosphatase 2A (PP2A), comprising formula (I). The compounds of the present disclosure are useful in treating, preventing, and/or ameliorating cancer, diabetes, autoimmune disease, solid organ transplant rejection, graft vs host disease, chronic obstructive pulmonary disease (COPD), non-alcoholic fatty liver disease, abdominal aortic aneurysm, chronic liver disease, heart failure, neurodegenerative disease, and cardiac hypertrophy.

公开(公告)号：US11858879B2

公开(公告)日：2024-01-02

申请号：US16625511

申请日：2018-06-22

申请人： City of Hope

发明人： Xiaochun Yu ,  Shih-Hsun Chen ,  Yate-Ching Yuan ,  Hongzhi Li ,  David Horne

IPC分类号： C07C251/86 ,  C07C311/17 ,  C07C311/29 ,  A61P35/00

CPC分类号： C07C251/86 ,  A61P35/00 ,  C07C311/17 ,  C07C311/29

摘要： Provided herein are, inter alia, compounds inhibiting poly(ADP-ribose) Glycohydrolase (PARG) in a cancer cell and methods of treating cancer using compounds of the invention.

公开(公告)号：US11096910B2

公开(公告)日：2021-08-24

申请号：US15746246

申请日：2016-07-22

申请人： OMEICOS THERAPEUTICS GMBH ,  BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM ,  MAX DELBRUCK-CENTRUM FUR MOLEKULARE MEDIZIN

发明人： Robert Fischer ,  Anne Konkel ,  Tim Wesser ,  Philipp Westphal ,  Wolf-Hagen Schunk ,  Christina Westphal ,  John Russell Falck

IPC分类号： A61P9/00 ,  A61K31/08 ,  A61K31/202 ,  A61K31/18 ,  C07C233/56 ,  C07C275/20 ,  C07C311/17 ,  C07D257/04 ,  C07C311/51 ,  C07D307/60 ,  C07D295/192 ,  C07D309/14 ,  C07D249/12 ,  C07D263/48 ,  A61K31/557 ,  A61P9/10 ,  A61P9/06 ,  A61P9/04 ,  A61K9/00 ,  A61K9/12 ,  A61K31/17 ,  A61K31/4196 ,  A61K31/5375

摘要： The present invention relates to compounds according to general formula (I) which are metabolically robust analogues of bioactive lipid mediators derived from omega-3 polyunsaturated fatty acids (n-3 PUFAs). The present invention further relates to compositions containing one or more of these compounds and to the use of these compounds or compositions for the treatment or prevention of cardiovascular diseases.

公开(公告)号：US11045476B2

公开(公告)日：2021-06-29

申请号：US16685555

申请日：2019-11-15

申请人： The Scripps Research Institute

发明人： Peter G. Schultz ,  Arnab K. Chatterjee ,  Shoutian Zhu ,  Joshua Payette ,  Hongchul Yoon ,  Baiyuan Yang

IPC分类号： A61K31/54 ,  C07C255/60 ,  A61K31/277 ,  A61K31/192 ,  C07D295/26 ,  A61K31/5375 ,  C07D317/66 ,  A61K31/36 ,  C07D319/08 ,  C07D233/64 ,  C07D261/14 ,  A61K31/42 ,  A61K45/06 ,  A61K31/196 ,  A61K31/255 ,  A61K31/4035 ,  C07C271/20 ,  C07C275/42 ,  C07C311/05 ,  C07C311/08 ,  C07C311/13 ,  C07C311/17 ,  C07C311/21 ,  C07C311/24 ,  C07C311/46 ,  C07C317/40 ,  C07C233/66 ,  C07C233/69 ,  C07C233/73 ,  C07C233/75 ,  C07C233/76 ,  C07C233/80 ,  C07C233/81 ,  C07C233/87 ,  C07C235/52 ,  C07C235/60 ,  C07C237/22 ,  C07C251/48 ,  A61K31/18 ,  A61K31/194 ,  A61K31/24 ,  A61K31/27 ,  A61K31/357 ,  A61K31/365 ,  A61K31/402 ,  A61K31/415 ,  A61K31/4164 ,  A61K31/426 ,  A61K31/433 ,  A61K31/44 ,  A61K31/495 ,  C07C235/84 ,  C07D207/27 ,  C07D209/46 ,  C07D209/48 ,  C07D213/79 ,  C07D231/40 ,  C07D277/46 ,  C07D285/135 ,  C07D307/88 ,  C07D317/28 ,  C07D319/18 ,  C12N5/077

摘要： Described herein are compounds and compositions for the amelioration of arthritis or joint injuries by inducing mesenchymal stem cells into chondrocytes.

公开(公告)号：US20200181078A1

公开(公告)日：2020-06-11

申请号：US16519590

申请日：2019-07-23

申请人： THE WISTAR INSTITUTE OF ANATOMY AND BIOLOGY

发明人： Troy E. Messick ,  Garry R. Smith ,  Allen B. Reitz ,  Paul M. Lieberman ,  Mark E. McDonnell ,  Yan Zhang ,  Venkata Velvadapu

IPC分类号： C07D207/327 ,  C07D401/10 ,  C07D401/04 ,  C07D333/54 ,  C07D307/79 ,  C07D277/30 ,  C07D249/06 ,  C07D231/12 ,  C07D215/14 ,  C07D213/74 ,  C07D213/64 ,  C07D211/70 ,  C07D207/16 ,  C07D207/14 ,  C07D207/12 ,  C07D207/08 ,  C07C317/44 ,  C07C229/64 ,  C07C65/28 ,  C07C65/19 ,  C07C63/66 ,  C07C53/18 ,  C07D213/55 ,  C07D295/155 ,  C07D209/08 ,  C07D487/04 ,  C07D471/04 ,  C07D417/10 ,  C07D409/10 ,  C07D239/26 ,  C07D403/10 ,  C07D235/06 ,  C07C317/14 ,  C07C311/17 ,  C07C311/16 ,  C07C311/08 ,  C07C235/58 ,  C07C233/65 ,  C07C233/64 ,  C07C233/11 ,  C07C217/84 ,  C07C211/27 ,  C07C255/55 ,  C07C255/54 ,  C07C229/56 ,  A61K31/44 ,  A61K31/192 ,  A61K31/496 ,  A61K31/4439 ,  A61K31/404

摘要： Pharmaceutical compositions of the invention comprise EBNA1 inhibitors useful for the treatment of diseases caused by EBNA1 activity such as cancer, infectious mononucleosis, chronic fatigue syndrome, multiple sclerosis, systemic lupus erythematosus and rheumatoid arthritis. Pharmaceutical compositions of the invention also comprise EBNA1 inhibitors useful for the treatment of diseases caused by latent Epstein-Barr Virus (EBV) infection. Pharmaceutical compositions of the invention also comprise EBNA1 inhibitors useful for the treatment of diseases caused by lytic Epstein-Barr Virus (EBV) infection.

公开(公告)号：US10421853B2

公开(公告)日：2019-09-24

申请号：US14766004

申请日：2014-03-04

申请人： CANON KABUSHIKI KAISHA

发明人： Kenji Kitagawa ,  Toshiki Ito

IPC分类号： C08K5/435 ,  C07C311/17 ,  C08F2/48 ,  G03F7/00 ,  H01L21/02 ,  H01L21/027 ,  B29C35/08 ,  B29C59/00 ,  B29C59/02 ,  B29D11/00 ,  C07C311/44 ,  G03F7/004 ,  B29K33/00 ,  B29L31/34

摘要： A photocurable composition excellent in the effect of reducing the mold releasing force even in a small amount of light exposure, and a photosensitive gas generating agent contained in the photocurable composition are provided.The photosensitive gas generating agent is a compound having a photostimulation responsive gas generating group to generate a gas by photostimulation, a perfluoroalkyl group and a polyalkyleneoxy group to link the photostimulation responsive gas generating group and the perfluoroalkyl group. The photocurable composition contains the photosensitive gas generating agent.

公开(公告)号：US10272081B2

公开(公告)日：2019-04-30

申请号：US15884044

申请日：2018-01-30

申请人： Aquinox Pharmaceuticals (Canada) Inc.

发明人： Lloyd F. Mackenzie ,  Thomas B. MacRury ,  Curtis Harwig ,  David Bogucki ,  Jeffery R. Raymond ,  Jeremy D. Pettigrew ,  Vladimir Khlebnikov ,  Rudong Shan

IPC分类号： A61K31/05 ,  A61K31/09 ,  A61K31/10 ,  A61K31/12 ,  C07C39/17 ,  C07C43/21 ,  C07C43/23 ,  C07C49/83 ,  C07C49/84 ,  C07C62/32 ,  C07C62/34 ,  A61K31/085 ,  A61K31/095 ,  A61K31/122 ,  A61K31/135 ,  A61K31/155 ,  A61K31/165 ,  A61K31/166 ,  A61K31/167 ,  A61K31/192 ,  A61K31/4965 ,  C07D405/12 ,  C07C49/835 ,  C07C43/215 ,  C07D241/24 ,  C07D213/81 ,  C07D249/08 ,  C07D295/112 ,  C07D213/75 ,  C07D295/215 ,  C07D211/66 ,  C07C311/18 ,  C07D213/82 ,  C07D213/89 ,  C07D233/64 ,  C07D401/12 ,  C07C233/76 ,  C07D213/38 ,  C07C255/47 ,  C07C275/26 ,  C07C275/64 ,  C07C279/16 ,  C07C311/07 ,  C07C311/17 ,  C07C317/22 ,  C07C217/84 ,  C07C323/20 ,  C07C225/20 ,  C07C233/26 ,  C07C233/28 ,  C07C233/31 ,  C07C233/32 ,  C07C233/60 ,  C07C235/82 ,  C07C237/08 ,  A61K31/277 ,  A61K31/4164 ,  A61K31/4196 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/443 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4465 ,  A61K31/495 ,  A61K31/496

摘要： Compounds of formula (I): where n, R1, R4a, R4b, R5, R7 and R8 are defined herein, or pharmaceutically acceptable salts thereof, are described herein. The disclosed compounds have activity as SHIP1 modulators, and thus may be used to treat any of a variety of diseases, disorders or conditions that would benefit from SHIP1 modulation. Compositions comprising a compound of formula (I) in combination with a pharmaceutically acceptable carrier or diluent are also disclosed, as are methods of SHIP1 modulation by administration of such compounds to an animal in need thereof.

公开(公告)号：US08835684B2

公开(公告)日：2014-09-16

申请号：US12840832

申请日：2010-07-21

申请人： Aslam A. Malik ,  Hasan Palandoken ,  Joy A. Stringer ,  Roland P. Carlson ,  John Leach ,  Thomas G. Archibald ,  Robert G. Miotke

发明人： Aslam A. Malik ,  Hasan Palandoken ,  Joy A. Stringer ,  Roland P. Carlson ,  John Leach ,  Thomas G. Archibald ,  Robert G. Miotke

IPC分类号： C07C303/38 ,  C07C269/06 ,  C07C303/40 ,  C07C311/17 ,  C07C311/18

CPC分类号： C07C269/06 ,  C07C303/40 ,  C07C311/18 ,  C07C271/20

摘要： The present invention provides a new process for the preparation of 2R,3S-N-isobutyl-N-(2-hydroxy-3-amino-4-phenylbutyl)-p-nitrobenzenesulfonylamide hydrochloride, wherein this compound is prepared directly from the chloromethylalcohol. Importantly, the process of the present invention results in higher yields of 2R,3S-N-isobutyl-N-(2-hydroxy-3-amino-4-phenylbutyl)-p-nitrobenzenesulfonylamide hydrochloride without sacrificing its purity. The processes of the present invention can be used to prepare not only the 2R,3S-derivative, but also the 2S,3S-, 2S,2R- and the 2R,3R-derivatives.

摘要翻译： 本发明提供了制备2R，3S-N-异丁基-N-（2-羟基-3-氨基-4-苯基丁基） - 对硝基苯磺酰胺盐酸盐的新方法，其中该化合物直接由氯甲基醇制备。 重要的是，本发明的方法导致2R，3S-N-异丁基-N-（2-羟基-3-氨基-4-苯基丁基） - 对硝基苯磺酰胺盐酸盐的产率较高，而不牺牲其纯度。 本发明的方法不仅可用于制备2R，3S-衍生物，而且可制备2S，3S-，2S，2R-和2R，3R-衍生物。

公开(公告)号：US20120270902A1

公开(公告)日：2012-10-25

申请号：US13372126

申请日：2012-02-13

申请人： Martin Neitzel ,  Jennifer Marugg

发明人： Martin Neitzel ,  Jennifer Marugg

IPC分类号： A61K31/18 ,  C07D211/56 ,  A61K31/445 ,  C07D213/42 ,  A61K31/4406 ,  C07D207/14 ,  A61K31/40 ,  C07D277/28 ,  A61K31/426 ,  C07D417/12 ,  A61K31/4439 ,  C07D317/46 ,  A61K31/357 ,  C07D319/16 ,  C07D311/58 ,  A61K31/353 ,  A61K31/4409 ,  C07D233/52 ,  A61K31/4168 ,  C07D307/52 ,  A61K31/341 ,  C07D209/14 ,  A61K31/4045 ,  A61P25/28 ,  A61P7/04 ,  C07C311/17 ,  A61P25/00 ,  C07D231/06 ,  A61K31/415 ,  C07C311/20

CPC分类号： C07D277/24 ,  C07C311/16 ,  C07C311/17 ,  C07C311/18 ,  C07C311/19 ,  C07C311/20 ,  C07C311/21 ,  C07C311/51 ,  C07C317/32 ,  C07C2601/02 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/18 ,  C07C2602/10 ,  C07C2602/42 ,  C07D209/14 ,  C07D211/58 ,  C07D231/06 ,  C07D307/52 ,  C07D307/81

摘要： The invention provides N-substituted benzenesulfonamides for use in treating or preventing cognitive disorders, such as Alzheimer's Disease. Compounds of particular interest are defined by Formula (I), wherein R1, R2, R3, R4, and R3′, are as described in the specification. The invention also encompasses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of treating cognitive disorders, including Alzheimer's disease using compounds of Formula (I).