公开(公告)号：US12077502B2

公开(公告)日：2024-09-03

申请号：US17871065

申请日：2022-07-22

申请人： PRAXIS PRECISION MEDICINES, INC.

发明人： Kiran Reddy ,  Margaret S. Lee ,  Gabriel Maurice Belfort ,  Sapna Makhija Garad ,  Mahesh Padval ,  Randall Wagner ,  Marion Wittmann

IPC分类号： C07D211/34 ,  A61K9/00 ,  A61K9/20 ,  A61K9/48 ,  A61K31/445 ,  A61K47/38 ,  A61P25/14 ,  C07D211/26

CPC分类号： C07D211/34 ,  A61K9/0053 ,  A61K9/2009 ,  A61K9/2013 ,  A61K9/2018 ,  A61K9/2054 ,  A61K9/4825 ,  A61K9/4858 ,  A61K9/4866 ,  A61K31/445 ,  A61K47/38 ,  A61P25/14 ,  C07D211/26 ,  C07B2200/13

摘要： Described herein, in part, are dosage forms and compositions useful for preventing and/or treating a disease or condition relating to aberrant function of a T-type calcium channel, such as epilepsy and epilepsy syndromes (e.g., absence seizures, juvenile myoclonic epilepsy, or a genetic epilepsy), tremor (e.g., essential tremor), and psychiatric disorder (e.g., mood disorders (e.g., major depressive disorder)). The present invention further comprises methods for modulating the function of a T-type calcium channel.

公开(公告)号：US11891369B2

公开(公告)日：2024-02-06

申请号：US16861166

申请日：2020-04-28

申请人： SRX Cardio, LLC

发明人： Anjali Pandey ,  Simeon Bowers ,  Thomas E. Barta ,  Jonathan William Bourne

IPC分类号： A61K31/4709 ,  C07D295/073 ,  C07D401/04 ,  C07D403/04 ,  C07D211/18 ,  C07D211/26 ,  C07D211/46 ,  C07D211/54 ,  C07D211/58 ,  C07D295/195 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D407/02 ,  C07D417/04 ,  C07D417/14 ,  C07D471/08

CPC分类号： C07D295/073 ,  C07D211/18 ,  C07D211/26 ,  C07D211/46 ,  C07D211/54 ,  C07D211/58 ,  C07D295/195 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D405/14 ,  C07D407/02 ,  C07D417/04 ,  C07D417/14 ,  C07D471/08

摘要： The present disclosure relates to novel compounds, methods, and compositions capable of binding to PCSK9, thereby modulating PCSK9 proprotein convertase enzyme activity, for treatment of a disease or condition mediated, at least in part, by PCSK9. The compounds of the disclosure include compounds Formula (I).

公开(公告)号：US11884654B2

公开(公告)日：2024-01-30

申请号：US17470464

申请日：2021-09-09

申请人： CHEMOCENTRYX, INC.

发明人： Trevor T. Charvat ,  Junfa Fan ,  Christopher W. Lange ,  Manmohan Reddy Leleti ,  Yandong Li ,  Venkat Reddy Mali ,  Jeffrey P. McMahon ,  Jay Powers ,  Sreenivas Punna ,  Ju Yang

IPC分类号： A01N43/00 ,  A61K31/00 ,  C07D413/06 ,  C07D401/04 ,  C07D401/06 ,  C07D403/06 ,  C07D405/06 ,  C07D417/04 ,  C07D211/56 ,  C07D295/135 ,  C07D211/62 ,  C07D211/26 ,  C07D211/70 ,  C07D241/04 ,  C07D207/16 ,  C07D211/34 ,  A61K31/451 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/495 ,  A61K31/496 ,  A61K31/5377

CPC分类号： C07D413/06 ,  A61K31/451 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/495 ,  A61K31/496 ,  A61K31/5377 ,  C07D207/16 ,  C07D211/26 ,  C07D211/34 ,  C07D211/56 ,  C07D211/62 ,  C07D211/70 ,  C07D241/04 ,  C07D295/135 ,  C07D401/04 ,  C07D401/06 ,  C07D403/06 ,  C07D405/06 ,  C07D417/04

摘要： Aniline compounds are provided which bind to CCR(4) and are useful for the treatment of diseases such as allergic diseases, autoimmune diseases, graft rejection and cancer.

公开(公告)号：US20220315556A1

公开(公告)日：2022-10-06

申请号：US17054491

申请日：2019-05-10

申请人： Glaxosmithkline Intellectual Property Development Limited

发明人： Jeffrey Michael Axten ,  Mui Cheung ,  Michael P. Demartino ,  Huiping Amy Guan ,  Yan Hu ,  Aaron Bayne Miller ,  Donghui Qin ,  Chengde Wu ,  Zhiliu Zhang ,  Xiaojuan Lin

IPC分类号： C07D401/14 ,  A61P11/00 ,  C07D401/12 ,  C07D211/26 ,  C07D487/08

摘要： This invention relates to novel compounds according to Formula (I) which are inhibitors of furin, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the treatment of fibrotic diseases, including pulmonary fibrosis, renal fibrosis, liver fibrosis, skin fibrosis, ocular fibrosis, cardiac fibrosis, and other miscellaneous fibrotic conditions. The disclosed compounds may also be useful for treating other furin-mediated conditions, including but not limited to, hypertension, cancer, infectious diseases, and genetic disorders (e.g., cystic fibrosis (CF)), and neurodegenerative disorders.

公开(公告)号：US11352322B2

公开(公告)日：2022-06-07

申请号：US16098341

申请日：2017-05-08

申请人： Jubilant Epicore LLC

发明人： Sridharan Rajagopal ,  Mahanandeesha S. Hallur ,  Purushottam Dewang ,  Kannan Murugan ,  Durga Prasanna Kumar C. H. ,  Pravin Iyer ,  Chandrika Mulakala ,  Dhanalakshmi Sivanandhan ,  Sreekala Nair ,  Mohd Zainuddin ,  Subramanyam Janardhan Tantry ,  Chandru Gajendran ,  Sriram Rajagopal

IPC分类号： C07D205/12 ,  A61P35/00 ,  C07C235/56 ,  C07C237/20 ,  C07C259/08 ,  C07D205/04 ,  C07D211/26 ,  C07D217/18 ,  C07D231/12 ,  C07D233/64 ,  C07D239/26 ,  C07D249/04 ,  C07D401/04 ,  C07D401/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/06 ,  C07D417/12 ,  C07D487/04 ,  C07D495/04 ,  C07D209/44 ,  A61K45/06

摘要： The present disclosure describes novel compounds of the general Formula (I), their analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts, pharmaceutical compositions, metabolites, and prodrugs thereof. These compounds can inhibit both LSD and HDAC and are useful as therpeautic or ameliorating agent for diseases that are involved in cellular growth such as malignant tumors, schizophrenia, Alzheimer's disease, parkinson's disease and the like.

公开(公告)号：US20210338653A1

公开(公告)日：2021-11-04

申请号：US17239726

申请日：2021-04-26

申请人： Neurocrine Biosciences, Inc.

发明人： Nicole Harriott ,  Nicholas Pagano

IPC分类号： A61K31/4545 ,  C07D401/12 ,  C07D211/40 ,  C07D211/26 ,  A61P25/28 ,  A61P25/18 ,  A61P25/16 ,  A61K31/444 ,  A61K31/496 ,  A61K31/506 ,  A61K31/519

摘要： Provided herein are small molecule compounds of the following formula (I): or a stereoisomer, tautomer, solvate, ester or pharmaceutically acceptable salt thereof, wherein A, B, C, Li, L2, Ri, R2, R3, R4, R5, w, x, y and z are as defined herein. Methods for treating diseases/disorders by antagonizing muscarinic receptors, including specifically antagonizing muscarinic receptor 4 (M4), are also disclosed. Such diseases/disorders are e.g. neurological diseases/disorders such as e.g. Alzheimer's Disease, Lewy Body Dementia and the cognitive deficits associated with schizophrenia, Parkinson's Disease, drug induced Parkinsonism, dyskinesias, dystonia, chorea, levodopa induced dyskinesia, cerebral palsy, progressive supranuclear palsy, and Huntington's disease. Preferred compounds are e.g. N-[2-(1-benzylpiperidin-4-yl)ethyl]-4-(pyrazin-2-yl)-piperazine-1-carboxamide derivatives and related compounds wherein the pyrazine has been replaced by e.g. pyridazine, pyrimidine, pyridine or phenyl.

公开(公告)号：US10982148B2

公开(公告)日：2021-04-20

申请号：US16486835

申请日：2018-02-02

申请人： JSR CORPORATION

发明人： Yuusuke Uesaka

IPC分类号： C09K19/56 ,  C07C69/54 ,  C07C219/34 ,  C07C309/46 ,  C07D207/09 ,  C07D209/88 ,  C07D211/26 ,  C07D213/74 ,  C07D239/26 ,  C07D295/096 ,  C08G73/10 ,  C08G77/20 ,  G02F1/1337

摘要： This liquid crystal display device is provided with: a pair of substrates which have conductive films, respectively; a liquid crystal layer which is arranged between the pair of substrates and contains a liquid crystal; and a liquid crystal control layer which is formed on the substrate-side interface of the liquid crystal layer by means of polymerization of a polymerizable monomer, and which controls the alignment of the liquid crystal. With respect to this liquid crystal display device, at least one of the pair of substrates is not provided with a liquid crystal alignment film, and the liquid crystal control layer contains a compound that has at least one partial structure which is selected from the group consisting of a fluorene structure-containing group, an aromatic amino group and a nitrogen-containing aromatic heterocyclic group.

公开(公告)号：US10961215B2

公开(公告)日：2021-03-30

申请号：US16341602

申请日：2017-10-09

申请人： Merck Sharp & Dohme Corp.

发明人： Michael T. Rudd ,  Zhaoyang Meng ,  Jenny Wai ,  David Jonathan Bennett ,  Edward J. Brnardic ,  Nigel J. Liverton ,  Shawn J. Stachel ,  Yongxin Han ,  Paul Tempest ,  Jiuxiang Zhu ,  Xuewang Xu

IPC分类号： C07D401/04 ,  C07D211/26 ,  C07D405/14

摘要： In its many embodiments, the present invention provides certain substituted N-aryl and N-heteroaryl piperidine compounds of the Formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, L, R4, L1, Q, R5 and R6 are as defined herein. The novel compounds of the invention, and pharmaceutically acceptable compositions comprising a compound thereof, may be useful as Liver X-β receptor (LXRβ) agonists, and may be useful for treating or preventing pathologies related thereto. Such pathologies include, but are not limited to, inflammatory diseases and diseases characterized by defects in cholesterol and lipid metabolism, such as Alzheimer's disease.

公开(公告)号：US10851123B2

公开(公告)日：2020-12-01

申请号：US16078585

申请日：2017-02-22

申请人： CONCENTRIC ANALGESICS, INC.

发明人： Craig Husfeld ,  Andrei W. Konradi

IPC分类号： A61P29/00 ,  C07F9/09 ,  C07D233/64 ,  C07D207/16 ,  C07C259/06 ,  C07C271/48 ,  C07C271/54 ,  C07C275/42 ,  C07C279/14 ,  C07C305/10 ,  C07C307/02 ,  C07C307/10 ,  C07C323/12 ,  C07C323/44 ,  C07C323/60 ,  C07C233/20 ,  C07C233/27 ,  C07C233/51 ,  C07F9/12 ,  C07F9/24 ,  C07F9/59 ,  C07D211/26 ,  C07D213/81 ,  C07D211/28 ,  C07D295/185 ,  C07D207/09

摘要： Described herein are compounds, pharmaceutical compositions and medicaments that include such compounds, and methods of using such compounds to modulate transient receptor potential vanilloid 1 receptor (TRPV1) activity.

公开(公告)号：US20200297710A1

公开(公告)日：2020-09-24

申请号：US16898667

申请日：2020-06-11

申请人： GlaxoSmithKline Intellectual Property Development Limited

发明人： Jeffrey Michael AXTEN ,  Mui CHEUNG ,  Michael P. DEMARTINO ,  Hilary Schenck EIDAM ,  Raghava Reddy KETHIRI ,  Biswajit KALITA

IPC分类号： A61K31/4468 ,  A61K31/438 ,  A61K31/439 ,  A61K31/445 ,  A61K31/454 ,  C07D211/32 ,  C07D211/58 ,  C07D211/66 ,  C07D403/12 ,  C07D417/12 ,  C07D471/08 ,  C07D498/10 ,  C07D211/26 ,  C07D211/60 ,  C07D401/04 ,  C07D211/56 ,  C07D211/62 ,  C07D401/12 ,  C07D209/52 ,  C07D405/12 ,  C07D451/04

摘要： The invention is directed to substituted piperidine derivatives. Specifically, the invention is directed to compounds according to Formula IIII: wherein A, B, X, Y, L1, L2, L3, R1, R2, R3, R4, R5, R6, R9, z2, z4, z5, and z6 are as defined herein, and salts thereof.The compounds of the invention are inhibitors of the ATF4 pathway and can be useful in the treatment of cancer, pre-cancerous syndromes and diseases associated with activated unfolded protein response pathways, such as Alzheimer's disease, spinal cord injury, traumatic brain injury, ischemic stroke, stroke, diabetes, Parkinson disease, Huntington's disease, Creutzfeldt-Jakob Disease, and related prion diseases, progressive supranuclear palsy, amyotrophic lateral sclerosis, myocardial infarction, cardiovascular disease, inflammation, fibrosis, chronic and acute diseases of the liver, chronic and acute diseases of the lung, chronic and acute diseases of the kidney, chronic traumatic encephalopathy (CTE), neurodegeneration, dementia, cognitive impairment, atherosclerosis, ocular diseases, arrhythmias, in organ transplantation and in the transportation of organs for transplantation. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting the ATF4 pathway and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.