公开(公告)号：US20210260048A1

公开(公告)日：2021-08-26

申请号：US17244065

申请日：2021-04-29

申请人： Bow River LLC

发明人： Sundar SRINIVASAN ,  Christina CHOW

IPC分类号： A61K31/4468 ,  A61K31/4995 ,  A61K31/519 ,  A61K31/4745 ,  A61K9/00 ,  A61K31/00 ,  A61K9/10 ,  A61K9/48 ,  A61K31/407 ,  A61P25/18 ,  A61K9/08 ,  A61K31/397 ,  A61K31/506 ,  A61K31/5395 ,  A61P35/02 ,  A61K9/20 ,  A61K31/498 ,  A61K31/5383 ,  A61P25/16 ,  A61K31/454 ,  A61K31/497 ,  A61P35/04

摘要： The present disclosure provides for methods of treating a patient with a CYP3A4 substrate drug, wherein the patient is treated with posaconazole. In some embodiments, the patient stops posaconazole treatment, waits for at least 2 days, and then is treated with the CYP3A4 substrate drug as soon as it is safe to do so. In some embodiments, treatment with the CYP3A4 substrate drug is delayed for about 2-42 days after stopping posaconazole. In some embodiments, the patient is treated with a reduced dose of the CYP3A4 substrate drug for about 2-42 days.

公开(公告)号：US11033540B2

公开(公告)日：2021-06-15

申请号：US16682041

申请日：2019-11-13

申请人： AUSPEX PHARMACEUTICALS, INC.

发明人： Andreas Sommer ,  Chengzhi Zhang ,  John Carter ,  John Charles Arthur ,  Margaret Bradbury ,  Thomas George Gant ,  Manouchehr Shahbaz

IPC分类号： A61K31/4745 ,  A61K31/473 ,  A61K31/519 ,  A61P25/14 ,  A61P25/28 ,  A61P25/18 ,  A61K9/00 ,  A61K9/16 ,  A61K9/20 ,  A61K9/28 ,  A61K9/48 ,  A61K9/50 ,  A61K45/06 ,  C07D455/06

摘要： The present invention relates to new pharmaceutical compositions comprising benzoquinoline compounds, and methods to inhibit vesicular monoamine transporter 2 (VMAT2) activity in a subject for the treatment of chronic hyperkinetic movement disorders.

公开(公告)号：US11033539B2

公开(公告)日：2021-06-15

申请号：US15773915

申请日：2016-11-04

申请人： Neurocrine Biosciences, Inc.

发明人： Nicole Harriott ,  Nicholas Pagano

IPC分类号： A61K31/445 ,  C07D211/14 ,  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, L1, L2, R2, R3, R4, R3, 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：US20210161880A1

公开(公告)日：2021-06-03

申请号：US17108623

申请日：2020-12-01

申请人： ACADIA Pharmaceuticals Inc.

发明人： Erin Foff

IPC分类号： A61K31/4468 ,  A61K31/496 ,  A61K31/7048 ,  A61K31/343 ,  A61K31/137 ,  A61K31/138 ,  A61K31/4525 ,  A61K31/15 ,  A61K31/135 ,  A61K31/165 ,  A61K31/445 ,  A61K31/55 ,  A61K31/27 ,  A61P25/28 ,  A61P25/18

摘要： This disclosure provides, in part, a method of decreasing the risk of relapse in a patient having dementia related psychosis, comprising administering to the patient an effective amount of pimavanserin daily. Also provided herein is a method of treating a dementia related psychosis in a patient in need thereof, comprising administering an effective amount of pimavanserin daily to the patient.

公开(公告)号：US11021448B2

公开(公告)日：2021-06-01

申请号：US16399134

申请日：2019-04-30

申请人： Hoffmann-La Roche Inc.

发明人： Alexander Flohr

IPC分类号： C07D243/24 ,  C07D243/22 ,  C07D401/04 ,  A61P25/28 ,  A61P25/18

摘要： The present invention provides compounds that are muscarinic M1 receptor positive allosteric modulators (PAM) and useful in the treatment of diseases, mediated by the muscarinic M1 receptor, such as Alzheimer's disease, cognitive impairment, schizophrenia, pain or sleep disorders, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances.

公开(公告)号：US20210154181A1

公开(公告)日：2021-05-27

申请号：US17150467

申请日：2021-01-15

申请人： Bow River LLC

发明人： Sundar SRINIVASAN ,  Christina CHOW

IPC分类号： A61K31/4468 ,  A61K31/498 ,  A61K31/5395 ,  A61P25/18 ,  A61K31/5383 ,  A61K31/506 ,  A61P35/02 ,  A61K31/4745 ,  A61K9/00 ,  A61K31/397 ,  A61K31/497 ,  A61K9/20 ,  A61K31/519 ,  A61P25/16 ,  A61K31/407 ,  A61K9/10 ,  A61K31/4995 ,  A61K31/00 ,  A61P35/04 ,  A61K9/08 ,  A61K31/454 ,  A61K9/48

摘要： The present disclosure provides for methods of treating a patient with a CYP3A4 substrate drug, wherein the patient is treated with posaconazole. In some embodiments, the patient stops posaconazole treatment, waits for at least 2 days, and then is treated with the CYP3A4 substrate drug as soon as it is safe to do so. In some embodiments, treatment with the CYP3A4 substrate drug is delayed for about 2-42 days after stopping posaconazole. In some embodiments, the patient is treated with a reduced dose of the CYP3A4 substrate drug for about 2-42 days.

公开(公告)号：US11013753B2

公开(公告)日：2021-05-25

申请号：US16083849

申请日：2017-03-10

申请人： CITY OF HOPE

发明人： Yanhong Shi

IPC分类号： C07H21/04 ,  A61K31/7105 ,  C07K14/705 ,  C12N15/85 ,  C12N15/113 ,  A61P25/18 ,  C12N15/115 ,  A61P25/24 ,  C12N5/07

摘要： Disclosed herein are methods of treating neurodevelopmental disorders such as schizophrenia (SCZ), bipolar disorder or depression. The methods entail inhibiting expression of miR-219 or overexpressing TLX thereby promoting proliferation of neural stem cells (NSCs) in the subjects.

公开(公告)号：US20210137941A1

公开(公告)日：2021-05-13

申请号：US16965269

申请日：2019-01-31

申请人： ZARODEX THERAPEUTICS LIMITED

发明人： Stephen JOLLES ,  Houman ASHRAFIAN ,  Duncan MCHALE

IPC分类号： A61K31/5513 ,  A61P25/18

摘要： This invention relates to the compound clozapine and its major metabolite norclozapine and prodrugs thereof and pharmaceutically acceptable salts and solvates thereof for use in the treatment or prevention of a pathogenic IgE driven B cell disease. The invention also provides pharmaceutical compositions containing such compounds.

公开(公告)号：US20210113553A1

公开(公告)日：2021-04-22

申请号：US16891160

申请日：2020-06-03

申请人： Neurocrine Biosciences, Inc.

发明人： Christopher F. O`Brien ,  Dimitri E. Grigoriadis

IPC分类号： A61K31/4745 ,  A61P25/18 ,  A61K9/20 ,  A61K9/48

摘要： Provided herein are methods for treating schizophrenia or schizoaffective disorder by administering to a subject in need thereof (,S)-2-amino-3-methyl-butyric acid (2R,3R,11bR)-3-isobutyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-yl ester, or an isotopic variant thereof, or a pharmaceutically acceptable salt or polymorph thereof.

公开(公告)号：US10980753B2

公开(公告)日：2021-04-20

申请号：US16445582

申请日：2019-06-19

申请人： LTS LOHMANN Therapie-Systeme AG

发明人： Patrick Mohr ,  René Rietscher ,  René Eifler ,  Olga Bourquain

IPC分类号： A61K9/70 ,  A61P25/18 ,  A61K31/407 ,  A61P9/12 ,  A61K9/00

摘要： The present invention relates to transdermal therapeutic systems (TTS) for the transdermal administration of asenapine comprising a self-adhesive layer structure containing a therapeutically effective amount of asenapine, such asenapine TTS for use in a method of treatment, processes of manufacture of such TTS as well as asenapine and transdermal therapeutic systems containing asenapine for use in a method of treatment and to a method of treating a human patient by transdermal administration of asenapine.