公开(公告)号：US20240358700A1

公开(公告)日：2024-10-31

申请号：US18758904

申请日：2024-06-28

申请人： Sumitomo Pharma Switzerland GmbH ,  Takeda Pharmaceutical Company Limited

发明人： Vijaykumar Reddy RAJASEKHAR ,  Brendan Mark JONHSON ,  David B. MACLEAN ,  Lynn SEELY ,  Paul N. MUDD, JR. ,  Hélène M. FAESSEL

IPC分类号： A61K31/501 ,  A61K9/00 ,  A61K31/4166 ,  A61K31/513 ,  A61P35/00

CPC分类号： A61K31/501 ,  A61K9/0053 ,  A61K31/4166 ,  A61K31/513 ,  A61P35/00

摘要： Methods for treating prostate cancer, including advanced prostate cancer, in a subject in need thereof, include administering once-daily to the subject, at least 80 mg of N-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxy-3-pyridazinyl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-N′-methoxyurea, or a corresponding amount of a pharmaceutically acceptable salt thereof. Another method includes: administering once-daily to the subject in need thereof, an oral load dose formulation having from 240 mg to 480 mg of N-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxy-3-pyridazinyl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-N′-methoxyurea, or a corresponding amount of a pharmaceutically acceptable salt thereof, and thereafter administering once-daily to the subject, an oral maintenance dose formulation having 80 mg to 160 mg of N-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxy-3-pyridazinyl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-N′-methoxyurea, or a corresponding amount of a pharmaceutically acceptable salt thereof.

公开(公告)号：US20240350487A1

公开(公告)日：2024-10-24

申请号：US18604264

申请日：2024-03-13

申请人： Altesa BioSciences, Inc.

发明人： Brett Paul GIROIR ,  John Michael CLERICI ,  Seth Allen RUDNICK ,  Katie LAESSIG ,  Katherine Elizabeth SQUIRES ,  Andrea True KELLY

IPC分类号： A61K31/501 ,  A61P31/16

CPC分类号： A61K31/501 ,  A61P31/16

摘要： The present disclosure describes methods of dosing vapendavir or a pharmaceutically acceptable salt thereof to treat subject in need thereof, thereby treating the respiratory enterovirus infection, wherein the respiratory enterovirus infection may be a respiratory enterovirus infection. The subject may further have an underlying condition, and the methods of the present disclosure may be useful in preventing or reducing acute exacerbations of the underlying condition in the subject. Pharmaceutical formulations of vapendavir are also disclosed.

公开(公告)号：US20240342199A1

公开(公告)日：2024-10-17

申请号：US18609635

申请日：2024-03-19

申请人： The Wistar Institute of Anatomy and Biology

发明人： Dario C. Altieri ,  Jagadish C. Ghosh

IPC分类号： A61K31/665 ,  A61K31/4745 ,  A61K31/501 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/585 ,  A61K31/66 ,  A61K45/06

CPC分类号： A61K31/665 ,  A61K31/4745 ,  A61K31/501 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/585 ,  A61K31/66 ,  A61K45/06

摘要： Pharmaceutical compositions for the treatment of cancer are provided. In one embodiment, the composition comprises Gamitrinib and a PI3K inhibitor selected from PX-866, AZD6482, LY294002, BEZ235, GSK458, GDC0941, ZSTK474, BKM120 and GSK2636771B. Methods of treating cancer are also provided.

公开(公告)号：US20240336624A1

公开(公告)日：2024-10-10

申请号：US18281855

申请日：2022-04-19

申请人： WIGEN BIOMEDICINE TECHNOLOGY (SHANGHAI) CO., LTD.

发明人： Yuli XIE ,  Yongcong LV ,  Lihui QIAN ,  Houxing FAN

IPC分类号： C07D498/04 ,  A61K31/496 ,  A61K31/497 ,  A61K31/498 ,  A61K31/4985 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5383 ,  C07D401/14 ,  C07D471/04

CPC分类号： C07D498/04 ,  A61K31/496 ,  A61K31/497 ,  A61K31/498 ,  A61K31/4985 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5383 ,  C07D401/14 ,  C07D471/04

摘要： Disclosed in the present invention are a PARP inhibitor containing a piperazine structure, a preparation method therefor and pharmaceutical use thereof. Particularly, the present invention relates to novel compounds of general formulas (1), (2), (3), (4) and (5) and/or a pharmaceutically acceptable salt thereof, a composition comprising the compounds of general formulas (1), (2), (3), (4) and (5) and/or the pharmaceutically acceptable salt thereof, a preparation method therefor and use thereof as a PARP inhibitor in the preparation of anti-tumor drugs.

公开(公告)号：US20240335441A1

公开(公告)日：2024-10-10

申请号：US18294129

申请日：2022-08-03

申请人： Jazz Pharmaceuticals Ireland Limited

发明人： Kimberly BABSON

IPC分类号： A61K31/501

CPC分类号： A61K31/501

摘要： This disclosure provides methods for treating a disease or disorder by administering pharmaceutical compounds. In particular, the disclosure relates to treating posttraumatic stress disorder in an individual in need thereof by administering a fatty acid amid hydrolase inhibitor or a pharmaceutically acceptable salt thereof.

公开(公告)号：US20240325385A1

公开(公告)日：2024-10-03

申请号：US18743948

申请日：2024-06-14

申请人： PEKING UNIVERSITY THIRD HOSPITAL

发明人： Lixiang XUE ,  Zhengyang GUO ,  Tengrui ZHANG ,  Yan WANG ,  Yan SUN ,  Yueqing GONG

IPC分类号： A61K31/496 ,  A61K31/501 ,  A61P35/00

CPC分类号： A61K31/496 ,  A61K31/501 ,  A61P35/00

摘要： Provided is a pharmaceutical composition for enhancing the anti-tumor effect of an EZH2 inhibitor. The pharmaceutical composition includes an EZH2 inhibitor and an SCD1 inhibitor. The SCD1 inhibitor enhances the effect of the EZH2 inhibitor on a solid tumor. Further provided are a related preparation of the pharmaceutical composition and the use thereof in the preparation of an anti-tumor drug.

公开(公告)号：US20240317713A1

公开(公告)日：2024-09-26

申请号：US18607834

申请日：2024-03-18

申请人： Pfizer Inc.

发明人： Michael Aaron Brodney ,  Jennifer Elizabeth Davoren ,  Amy Beth Dounay ,  Ivan Viktorovich Efremov ,  David Lawrence Firman Gray ,  Michael Eric Green ,  Jaclyn Louise Henderson ,  Chewah Lee ,  Scot Richard Mente ,  Steven Victor O'Neil ,  Bruce Nelsen Rogers ,  Lei Zhang

IPC分类号： C07D401/14 ,  A61K31/444 ,  A61K31/501 ,  A61K31/506 ,  A61K31/513 ,  A61P25/18 ,  A61P25/28 ,  C07D401/12 ,  C07D403/12 ,  C07D405/14

CPC分类号： C07D401/14 ,  A61K31/444 ,  A61K31/501 ,  A61K31/506 ,  A61K31/513 ,  A61P25/18 ,  A61P25/28 ,  C07D401/12 ,  C07D403/12 ,  C07D405/14

摘要： The present invention provides, in part, compounds of Formula I:




and pharmaceutically acceptable salts thereof; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds or salts, and their uses for treating D1-mediated (or D1-associated) disorders including, e.g., schizophrenia (e.g., its cognitive and negative symptoms), cognitive impairment (e.g., cognitive impairment associated with schizophrenia, AD, PD, or pharmacotherapy therapy), ADHD, impulsivity, compulsive gambling, overeating, autism spectrum disorder, MCI, age-related cognitive decline, dementia, RLS, Parkinson's disease, Huntington's chorea, anxiety, depression, MDD, TRD, bipolar disorder, chronic apathy, anhedonia, chronic fatigue, post-traumatic stress disorder, seasonal affective disorder, social anxiety disorder, post-partum depression, serotonin syndrome, substance abuse and drug dependence, drug abuse relapse, Tourette's syndrome, tardive dyskinesia, drowsiness, excessive daytime sleepiness, cachexia, inattention, sexual dysfunction, migraine, SLE, hyperglycemia, atherosclerosis, dislipidemia, obesity, diabetes, sepsis, post-ischemic tubular necrosis, renal failure, hyponatremia, resistant edema, narcolepsy, hypertension, congestive heart failure, postoperative ocular hypotonia, sleep disorders, and pain.

公开(公告)号：US20240308980A1

公开(公告)日：2024-09-19

申请号：US18550303

申请日：2022-03-14

申请人： Merck Sharp & Dohme LLC

发明人： Kaleen Konrad Childers ,  J. Michael Ellis ,  Peter H. Fuller ,  Anmol Gulati ,  Hakan Gunaydin ,  Solomon D. Kattar ,  Ravi Kurukulasuriya ,  Joey L. Methot ,  Gregori J. Morriello ,  Santhosh Neelamkavil ,  Blair T. Lapointe ,  Vladimir Simov ,  Charles S. Yeung

IPC分类号： C07D401/14 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5377 ,  C07D405/14 ,  C07D413/14 ,  C07D491/048 ,  C07D491/107 ,  C07D498/10

CPC分类号： C07D401/14 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5377 ,  C07D405/14 ,  C07D413/14 ,  C07D491/048 ,  C07D491/107 ,  C07D498/10

摘要： The present invention is directed to certain 2-aminoquinzaoline derivatives of Formula (I): (I) and pharmaceutically acceptable salts thereof, wherein A, R1, R2, and R3 are as defined herein, which are potent inhibitors of LRRK2 kinase and may be useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease and other diseases and disorders described herein. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which LRRK-2 kinase is involved.

公开(公告)号：US20240308973A1

公开(公告)日：2024-09-19

申请号：US18598312

申请日：2024-03-07

申请人： Zoetis Services LLC

发明人： Richard A. EWIN ,  Michael P. CURTIS ,  Todd M. MADDUX ,  Graham M. KYNE

IPC分类号： C07D401/04 ,  A61K31/433 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/501 ,  A61K31/506 ,  A61K31/549 ,  A61K31/55 ,  A61K45/06 ,  C07D401/14 ,  C07D403/04 ,  C07D417/04 ,  C07D417/14 ,  C07D471/04

CPC分类号： C07D401/04 ,  A61K31/433 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/501 ,  A61K31/506 ,  A61K31/549 ,  A61K31/55 ,  A61K45/06 ,  C07D401/14 ,  C07D403/04 ,  C07D417/04 ,  C07D417/14 ,  C07D471/04

摘要： The invention describes novel PDE3 inhibitors for treating a cardiovascular disease including myxomatous mitral valve disease, congestive heart failure and/or asymptomatic heart failure in animals, particularly canines.

公开(公告)号：US20240307388A1

公开(公告)日：2024-09-19

申请号：US18501268

申请日：2023-11-03

申请人： LIPIDIO PHARMACEUTICALS, INC.

发明人： Nigel R.A Beeley ,  John Gordon Foulkes ,  Kieran George Mooney ,  Charles Rodney Greenaway Evans ,  Keith Arthur Johnson ,  Howard G. Welgus ,  Celia P. Jenkinson ,  James R. Hauske

IPC分类号： A61K31/501 ,  A61K9/00 ,  A61K9/06 ,  A61K31/40 ,  A61K31/4439 ,  A61K45/06 ,  A61K47/02 ,  A61K47/10 ,  A61K47/14 ,  A61K47/18 ,  A61K47/32

CPC分类号： A61K31/501 ,  A61K31/40 ,  A61K31/4439 ,  A61K47/02 ,  A61K47/10 ,  A61K47/14 ,  A61K47/183 ,  A61K47/32 ,  A61K9/0014 ,  A61K9/06 ,  A61K45/06

摘要： Pharmaceutical carriers which provide an environment of physical and chemical stability comprising a therapeutically effective amount of an active pharmaceutical ingredient (API) compound of structure I, one or more antioxidants, one or more chelators and a vehicle base comprising water and one or more pharmaceutically acceptable non-aqueous solvents, one or more absorption enhancers, one or more gelling agents and one or more pH buffering agents are described.