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1. 发明申请

US20190247331A1 COMPOSITION AND METHOD FOR TREATING NEUROLOGICAL DISEASE 审中-公开
公开(公告)号：US20190247331A1
公开(公告)日：2019-08-15
申请号：US16268373
申请日：2019-02-05
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 , A61K9/00 , A61P25/16 , A61K9/20 , A61K45/06
CPC分类号： A61K31/13 , A61K9/0004 , A61K9/20 , A61K45/06 , 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.

2. 发明申请

US20190247321A1 DONEPEZIL TRANSDERMAL DELIVERY SYSTEM 审中-公开
公开(公告)号：US20190247321A1
公开(公告)日：2019-08-15
申请号：US16392544
申请日：2019-04-23
申请人： Corium, Inc.
发明人： Eun Soo LEE , Amit K. JAIN , Parminder SINGH
IPC分类号： A61K9/70 , A61K47/10 , A61K47/12 , A61K47/32 , A61K31/27 , A61K31/18 , A61K31/137 , A61K31/13 , A61K31/445 , C08K5/00 , A61K47/02 , A61K31/00
CPC分类号： A61K9/7038 , A61K9/7023 , A61K9/7053 , A61K9/7061 , A61K9/7084 , A61K9/7092 , A61K31/00 , A61K31/045 , A61K31/13 , A61K31/137 , A61K31/18 , A61K31/27 , A61K31/445 , A61K47/02 , A61K47/10 , A61K47/12 , A61K47/32 , C08K5/0016
摘要： A transdermal delivery system for systemic delivery of donepezil is described, where the system comprises an adhesive matrix drug reservoir layer comprised of a copolymer of acrylic acid/vinyl acetate, triethyl citrate, and donepezil base generated in situ by reaction of donepezil HCl and an alkaline salt. The system is provided for treatment of Alzheimer's disease, and achieves transdermal delivery of the therapeutic agent at steady state that is bioequivalent to administration of the therapeutic agent orally.

3. 发明申请

US20190247320A1 METHODS FOR TREATING ALZHEIMER'S DISEASE WITH DONEPEZIL TRANSDERMAL SYSTEM 审中-公开
公开(公告)号：US20190247320A1
公开(公告)日：2019-08-15
申请号：US16392513
申请日：2019-04-23
申请人： Corium, Inc.
发明人： Eun Soo LEE , Amit K. JAIN , Parminder SINGH
IPC分类号： A61K9/70 , A61K47/10 , A61K47/12 , A61K47/32 , A61K31/27 , A61K31/18 , A61K31/137 , A61K31/13 , A61K31/445 , C08K5/00 , A61K47/02 , A61K31/00
CPC分类号： A61K9/7038 , A61K9/7023 , A61K9/7053 , A61K9/7061 , A61K9/7084 , A61K9/7092 , A61K31/00 , A61K31/045 , A61K31/13 , A61K31/137 , A61K31/18 , A61K31/27 , A61K31/445 , A61K47/02 , A61K47/10 , A61K47/12 , A61K47/32 , C08K5/0016
摘要： A transdermal delivery system for systemic delivery of donepezil is described, where the system comprises an adhesive matrix drug reservoir layer comprised of a copolymer of acrylic acid/vinyl acetate, triethyl citrate, and donepezil base generated in situ by reaction of donepezil HCl and an alkaline salt. The system is provided for treatment of Alzheimer's disease, and achieves transdermal delivery of the therapeutic agent at steady state that is bioequivalent to administration of the therapeutic agent orally.

4. 发明申请

US20190111054A1 NOVEL COMBINATORIAL THERAPIES OF NEUROLOGICAL DISORDERS 审中-公开
公开(公告)号：US20190111054A1
公开(公告)日：2019-04-18
申请号：US16074783
申请日：2017-02-03
申请人： PHARNEXT
发明人： DANIEL COHEN , SERGUEI NABIROTCHKIN , RODOLPHE HAJJ
IPC分类号： A61K31/496 , A61K31/185 , A61K31/197 , A61K31/445 , A61K31/13 , A61K31/473 , A61K31/27 , A61K31/55 , A61K31/198 , A61P25/00 , A61P25/16 , A61P25/28
CPC分类号： A61K31/496 , A61K31/13 , A61K31/185 , A61K31/197 , A61K31/198 , A61K31/27 , A61K31/445 , A61K31/473 , A61K31/55 , A61P25/00 , A61P25/16 , A61P25/28 , A61K2300/00
摘要： The present invention relates to combinations and methods for the treatment of neurological disorders related Amyloid beta toxicity and/or neuronal death. More specifically, the present invention relates to novel combinatorial therapies of Alzheimer's disease, Alzheimer's disease related disorders, Parkinson's disease, Lewy body dementia, multiple system atrophy and other related synucleinopathies, Huntington's disease, peripheral neuropathies, alcoholism or alcohol withdrawal, neurological manifestations of drug abuse or drug abuse withdrawal, amyotrophic lateral sclerosis, multiple sclerosis, spinal cord injury, epilepsy, traumatic brain injury or brain ischemic events based on 3-phenylsulfonyl-8-(piperazin-1-yl) quinolone and baclofen and/or acamprosate.

5. 发明申请

US20180369168A1 METHOD FOR TREATING HYPERHIDROSIS 审中-公开
公开(公告)号：US20180369168A1
公开(公告)日：2018-12-27
申请号：US16019690
申请日：2018-06-27
申请人： Atacama Therapeutics, Inc.
发明人： Merouane Bencherif
IPC分类号： A61K31/13 , A61K9/00 , A61K9/20
CPC分类号： A61K31/13 , A61K9/0053 , A61K9/20
摘要： The present invention relates to dexmecamylamine and the use of dexmecamylamine, substantially free of exo-R-mecamylamine, in the treatment of hyperhidrosis.

6. 发明申请

US20180344751A1 Broad Spectrum Antiviral and Methods of Use 审中-公开
公开(公告)号：US20180344751A1
公开(公告)日：2018-12-06
申请号：US15854184
申请日：2017-12-26
申请人： The Burlington HC Research Group, Inc.
发明人： Dale M. Walker , Adriana Elisa Kajon , Vernon E. Walker
IPC分类号： A61K31/661 , A61K45/06 , A61K31/13 , A61K31/66
CPC分类号： A61K31/661 , A61K31/13 , A61K31/66 , A61K45/06
摘要： A method for the prevention or treatment of Influenza virus infection or Adenovirus infection by administering an effective amount of a compound of Formula (I), Formula (II), or similar compound to an individual in need is provided.

7. 发明申请

US20180318288A1 GLUTAMATE AGENTS IN THE TREATMENT OF MENTAL DISORDERS 审中-公开
公开(公告)号：US20180318288A1
公开(公告)日：2018-11-08
申请号：US16031250
申请日：2018-07-10
申请人： YALE UNIVERSITY
发明人： Vladimir Coric , John H. Krystal , Gerard Sanacora
IPC分类号： A61K31/485 , A61K31/43 , A61K31/545 , A61K31/428 , A61K31/425 , A61K31/13 , A61K31/198 , A61K45/06
CPC分类号： A61K31/485 , A61K31/13 , A61K31/198 , A61K31/425 , A61K31/428 , A61K31/43 , A61K31/545 , A61K45/06 , A61K2300/00
摘要： Methods of treating mental disorders, including anxiety disorders such as obsessive-compulsive disorder, are provided. The methods comprise administering an effective amount of a glutamate modulator to an individual in need thereof. Also provided are methods of enhancing the activity of a serotonin reuptake inhibitor (SRI) comprising co-administering a glutamate modulator and a serotonin reuptake inhibitor. Pharmaceutical composition comprising a serotonin reuptake inhibitor and a glutamate modulator are also provided.

8. 发明申请

US20180280344A1 Conjugate of Memantine and Arctigenin, and Composition and Use Thereof 审中-公开
公开(公告)号：US20180280344A1
公开(公告)日：2018-10-04
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： A61K31/365 , A61K31/13 , A61K47/54 , A61K45/06 , A61P25/28
CPC分类号： A61K31/365 , A61K31/13 , A61K31/445 , A61K31/473 , A61K31/4748 , A61K45/06 , A61K47/542 , A61K47/55 , A61P25/28 , A61K2300/00
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.

9. 发明申请

US20180243244A1 Prevention and Treatment of Neurodegenerative Diseases Through Autophagy Activity Mediated by A Synthetic Ligand or Arginylated BIP Binding to the P62 ZZ Domain 审中-公开
公开(公告)号：US20180243244A1
公开(公告)日：2018-08-30
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 , A61P25/28
CPC分类号： A61K31/138 , A61K31/122 , A61K31/13 , A61K38/05 , A61K38/10 , A61K38/16 , A61P25/28 , Y02A50/401
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)}).

10. 发明授权

US10058523B2 Benzoquinone derivative E3330 in combination with chemotherapeutic agents for the treatment of cancer and angiogenesis 有权
公开(公告)号：US10058523B2
公开(公告)日：2018-08-28
申请号：US14690973
申请日：2015-04-20
申请人： Indiana University Research and Technology Corporation
发明人： Mark R. Kelley
IPC分类号： A61K31/201 , A61K33/24 , A61K31/7068 , A61K31/198 , A61K39/395 , A61K31/454 , A61K31/195 , A61K45/06 , A61K31/122 , A61K31/13 , A61K31/282 , A61K31/203
CPC分类号： A61K31/201 , A61K31/122 , A61K31/13 , A61K31/195 , A61K31/198 , A61K31/203 , A61K31/282 , A61K31/454 , A61K31/7068 , A61K33/24 , A61K39/3955 , A61K45/06 , A61K2300/00
摘要： Disclosed are novel methods for the therapeutic treatment of cancer and angiogenesis. The enzyme Ape1/Ref-1, via its redox function, enhances the DNA binding activity of transcription factors that are associated with the progression of cancer. The present invention describes the use of agents to selectively inhibit the redox function of Ape1/Ref-1 and thereby reduce tumor cell growth, survival, migration and metastasis. In addition, Ape1/Ref-1 inhibitory activity is shown to augment the therapeutic effects of other therapeutics and protect normal cells against toxicity. Further, Ape1/Ref-1 inhibition is shown to decrease angiogenesis, for use in the treatment of cancer as well other pathologic conditions of which altered angiogenesis is a component.

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