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91. 发明申请

US20200022943A1 Anavex2-73 for the Treatment of Alzheimer's Disease 审中-公开
公开(公告)号：US20200022943A1
公开(公告)日：2020-01-23
申请号：US16585495
申请日：2019-09-27
申请人： ANAVEX LIFE SCIENCES CORP.
发明人： Marco Cecchi
IPC分类号： A61K31/341 , A61K31/13 , A61K31/27 , A61K31/445 , A61K31/55 , A61K45/06
摘要： Composition and method for treatment of Alzheimer's disease that includes ANAVEX2-73. Method of treatment of Alzheimer's disease using pharmaceutical compositions comprising ANAVEX2-73 according to an intermittent dosage regimen.

92. 发明授权

US10519107B2 Sulfonamide compounds and their use as STAT5 inhibitors 有权
公开(公告)号：US10519107B2
公开(公告)日：2019-12-31
申请号：US15315324
申请日：2015-05-29
申请人： Governing Council of the University of Toronto
发明人： Patrick Thomas Gunning , Abbarna A. Cumaraswamy , Andrew Martin Lewis , Mulu Geletu-Heye
IPC分类号： C07C311/19 , C07D233/64 , C07D307/14 , C07D307/52 , C07D333/20 , A61K31/63 , A61K31/13 , A61K31/025
摘要： The present disclosure relates to compounds having the Formula (Formula (I)) which are inhibitors of STAT5.

93. 发明授权

US10500172B2 Composition and method for treating neurological disease 有权
公开(公告)号：US10500172B2
公开(公告)日：2019-12-10
申请号：US16250686
申请日：2019-01-17
申请人： Osmotica Kereskedelmi és Szolgáltató Korlátolt Felelõsségû Társaság
发明人： Glenn A. Meyer , Joaquina Faour , Ana Cristina Pastini , Marcelo Fernando Befumo
IPC分类号： A61K31/13 , A61P25/14 , A61K9/00 , A61K9/20 , A61P25/16
CPC分类号： A61K31/13 , A61K9/0004 , A61K9/0053 , A61K9/20 , A61P25/14 , A61P25/16
摘要： The present disclosure is directed to methods of treating neurological disorders in a patient such as Parkinson's disease, drug-induced extrapyramidal reactions, and/or levodopa-induced dyskinesia comprising administering to the patient once daily in the morning a pharmaceutical composition comprising about 50 mg to about 400 mg of extended-release amantadine or a pharmaceutically acceptable salt thereof.

94. 发明授权

US10485774B2 Enterically coated cysteamine, cystamine and derivatives thereof 有权
公开(公告)号：US10485774B2
公开(公告)日：2019-11-26
申请号：US15922520
申请日：2018-03-15
申请人： The Regents of the University of California
发明人： Ranjan Dohil , Jerry Schneider
IPC分类号： A61K31/194 , A61K9/28 , A61K31/13 , A61K31/145 , A61K9/00 , A61K9/48 , A61K9/50 , A61K9/16
CPC分类号： A61K31/194 , A61K9/0053 , A61K9/1605 , A61K9/284 , A61K9/288 , A61K9/2846 , A61K9/2866 , A61K9/2873 , A61K9/4808 , A61K9/5005 , A61K9/5026 , A61K9/5042 , A61K9/5047 , A61K9/5057 , A61K9/5063 , A61K31/13 , A61K31/145
摘要： The disclosure provides oral cysteamine and cystamine formulations useful for treating cystinosis and neurodegenerative diseases and disorders. The formulations provide controlled release compositions that improve quality of life and reduced side-effects.

95. 发明申请

US20190350927A1 COMBINATIONS COMPRISING 3-PHENYLSULFONYL-8-PIPERAZINYL-1YL-QUINOLINE 审中-公开
公开(公告)号：US20190350927A1
公开(公告)日：2019-11-21
申请号：US16218186
申请日：2018-12-12
申请人： Axovant Sciences GmbH
发明人： Tsu Tshen CHUANG , Ann Jacqueline HUNTER , David John VIRLEY
IPC分类号： A61K31/496 , A61K31/5513 , A61K31/00 , A61K31/4525 , A61K45/06 , A61K31/519 , A61K31/13
摘要： The combination of 3-phenylsulfonyl-8-piperazinyl-1yl-quinoline or a pharmaceutically acceptable salt thereof with a second therapeutic agent, and its use for the treatment of a) psychiatric disorders with prominent cognitive deficits e.g. chronic PTSD (Post traumatic stress disorder); b) non-degenerative disorders with prominent cognitive deficits e.g. MS (multiple Sclerosis), post-chemotherapy, post-CABG (Coronary artery bypass graft), post-stroke; and/or c) paediatric disorders e.g. autism, mental retardation and learning disabilities, in particular for the treatment of schizophrenia.

96. 发明授权

US10441565B2 Conjugate of memantine and arctigenin, and composition and use thereof 有权
公开(公告)号：US10441565B2
公开(公告)日：2019-10-15
申请号：US15756342
申请日：2015-08-31
申请人： Shenzhen Qingyaqirui Bio-Tech Co., Ltd.
发明人： Haifeng Sun , Zhiyuan Zhu , Jun Liu , Wei Yan , Ding Zhang , Jing Yang
IPC分类号： A61K31/13 , A61K31/365 , A61K47/54 , A61P25/28 , A61K45/06 , A61K47/55 , A61K31/445 , A61K31/473 , A61K31/4748
摘要： Provided are a conjugate of memantine and arctigenin, and a pharmaceutical composition comprising the conjugate. The conjugate can treat diseases associated with Aβ or Tau protein pathways, such as Alzheimer's disease or Parkinson's disease.

97. 发明申请

US20190307707A1 METHODS OF ADMINISTERING AMANTADINE 审中-公开
公开(公告)号：US20190307707A1
公开(公告)日：2019-10-10
申请号：US16188770
申请日：2018-11-13
申请人： Adamas Pharma, LLC
发明人： Gregory T. WENT , Timothy J. FULTZ , Natalie MCCLURE
IPC分类号： A61K31/13 , A61K9/50
摘要： Methods of nighttime administration of amantadine to reduce sleep disturbances in patient undergoing treatment with amantadine are described, as well as compositions of extended release amantadine that are suitable for nighttime administration.

98. 发明授权

US10421723B2 2,3-diacylated, 2- and 3-mono-acylated alkylated imino sugars exhibiting glucosidase inhibition and their method of use 有权
公开(公告)号：US10421723B2
公开(公告)日：2019-09-24
申请号：US15492652
申请日：2017-04-20
申请人： Baruch S. Blumberg Institute
发明人： Yanming Du , Jinhong Chang , Timothy Michael Block
IPC分类号： C07D211/40 , C07D211/36 , C07D419/12 , A61K31/45 , A61K31/13
摘要： Described herein are alkylated imino sugars derivatives having a disease-modifying action in the treatment of diseases associated with glucosidase activity that include viral hemorrhagic fevers and other enveloped viruses, and any other diseases involving glucosidase activity.

99. 发明申请

US20190274955A1 PAMOATE SALTS AND METHODS OF USE 审中-公开
公开(公告)号：US20190274955A1
公开(公告)日：2019-09-12
申请号：US16358391
申请日：2019-03-19
申请人： Zi-Qiang Gu
发明人： Zi-Qiang Gu
IPC分类号： A61K9/00 , C07C271/44 , C07C211/38 , C07C65/11 , C07D211/32 , A61K31/27 , A61K31/13 , A61K31/445
摘要： The composition containing a pamoate salt of donepezil, the method of preparation and the use thereof are disclosed.

100. 发明授权

US10391067B2 Prevention and treatment of neurodegenerative diseases through autophagy activity mediated by a synthetic ligand or arginylated BIP binding to the P62 ZZ domain 有权
公开(公告)号：US10391067B2
公开(公告)日：2019-08-27
申请号：US15753026
申请日：2016-07-15
申请人： Seoul National University R&DB Foundation , Korea Research Institute of Bioscience and Biotechnology
发明人： Yong Tae Kwon , Bo Yeon Kim , Hyunjoo Cha , Young Dong Yoo , Ji-eun Yu
IPC分类号： A61K31/138 , A61K38/05 , A61K38/10 , A61K38/16 , A61K31/122 , A61K31/13 , A61P25/28
摘要： The pharmacokinetics and key technologies of the present invention are summarized in FIG. 1. Particularly, malignant misfolded proteins such as mutant huntingtin and alpha-synuclein are coagulated and grow into oligomeric coagulum ({circle around (1)}, {circle around (2)}, fibrillar coagulum ({circle around (3)}) and eventually inclusion body ({circle around (4)}). Young neurons produce a large amount of Nt-Arg through N-terminal arginylation ({circle around (5)}) of vesicle chaperones such as BiP secreted into the cytoplasm, and then arginylated BiP (R-BiP) is secreted binds to the misfolded proteins ({circle around (6)}). As a ligand, the Nt-Arg of R-BiP binds to the p62 ZZ domain ({circle around (7)}), and the normally inactivated closed form of p62 is changed to an open form, leading to structural activation ({circle around (8)}). As a result, PB1 and LC3-binding domains are exposed. The PB1 domain induces oligomerization ({circle around (9)}), leading to the concentration as a p62 body ({circle around (10)}) that is a coagulum capable of being degraded by autophagy. Then, p62 binds to LC3, which is protruding from the autopagosomal membranes, leading to the completion of autophagy targeting ({circle around (11)}) and lysosomal proteolysis. Since autophagy proteolysis including steps ({circle around (5)})-({circle around (11)}) is strong in young neurons, cytotoxic protein coagulums ({circle around (1)}-{circle around (5)}) do not accumulate. However in aged neurons, autophagy proteolysis including steps {circle around (5)}-{circle around (11)} is weakened, and protein coagulums ({circle around (1)}-{circle around (5)}) accumulate and become cytotoxic. In this invention, p62 is intentionally activated ({circle around (12)}, {circle around (13)}) by using low mass ligands of the p62 ZZ domain to effectively remove huntingtin and alpha-synuclein protein coagulums. Particularly, in step {circle around (12)}, p62 ligated with a ligand accelerates the oligomerization of p62-R-BiP-misfolded protein ({circle around (9)}) and the formation of autophagy coagulum ({circle around (10)}). In step ({circle around (13)}), the ligand-p62 conjugate acts as an autophagy activator ({circle around (14)}) to induce the synthesis of LC3 and the conversion of LC3-I into LC3-II in order to accelerate the formation of autophagosomes ({circle around (15)}).

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