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1.
公开(公告)号:US20240285584A1
公开(公告)日:2024-08-29
申请号:US18478718
申请日:2023-09-29
申请人: Allergan, Inc.
IPC分类号: A61K31/417 , A61K31/17 , A61K31/197 , A61K31/198 , A61K31/216 , A61K31/4045 , C07C275/30 , C07C317/42 , C07C317/50 , C07C323/44 , C07C323/60 , C07D209/20 , C07D233/64 , C07K5/062 , C07K5/072 , C07K5/078
CPC分类号: A61K31/417 , A61K31/17 , A61K31/197 , A61K31/198 , A61K31/216 , A61K31/4045 , C07C275/30 , C07C317/42 , C07C317/50 , C07C323/44 , C07C323/60 , C07D209/20 , C07D233/64 , C07K5/06017 , C07K5/06034 , C07K5/06052 , C07K5/0606 , C07K5/06113 , C07K5/06147 , C07K5/06156 , Y02A50/30
摘要: The present invention relates to novel amide derivatives of N-urea substituted amino acids, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.
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公开(公告)号:US20240091213A1
公开(公告)日:2024-03-21
申请号:US18200950
申请日:2023-05-23
申请人: DANA-FARBER CANCER INSTITUTE, INC. , THE GENERAL HOSPITAL CORPORATION d/b/a MASSACHUSETTS GENERAL HOSPITAL
发明人: Nathanael S. Gray , Stephen J. Haggarty , Quan Cai , Tinghu Zhang , Maria Catarina Telo Baptista Lima da Silva , Fleur M. Ferguson
IPC分类号: A61K31/4545 , A61P25/28 , A61K31/437 , A61K38/05 , A61K51/04 , C07D471/04 , C07K5/062 , G01N33/534 , G01N33/68
CPC分类号: A61K31/4545 , A61P25/28 , A61K31/437 , A61K38/05 , A61K51/0455 , C07D471/04 , C07K5/06034 , G01N33/534 , G01N33/6896
摘要: Provided herein are bifunctional compounds that bind tau protein and/or promote targeted ubiquitination for the degradation of tau protein. In particular, provided are compounds that can bind tau protein, a protein whose aggregation is implicated in a variety of neurodegenerative disease (e.g., tauopathies), and can promote its degradation by recruiting an E3 ubiquitin ligase (e.g., Cereblon), which can ubiquitinate tau protein, marking it for proteasomal degradation. Also provided are radiolabeled forms of the bifunctional compounds, pharmaceutical compositions comprising the bifunctional compounds, methods of detecting and/or diagnosing neurological disorders, methods of detecting and/or diagnosing pathological aggregation of tau protein (e.g., in the central nervous system), methods of treating and/or preventing neurological disorders, and methods of promoting the degradation of tau protein by E3 ubiquitin ligase activity in a subject by administering a compound or composition described herein.
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公开(公告)号:US20190233471A1
公开(公告)日:2019-08-01
申请号:US16231312
申请日:2018-12-21
发明人: Wolfgang Richter
IPC分类号: C07K5/078 , C07K5/062 , C07D417/12 , C07K5/02 , C07D277/56 , C07D417/14
CPC分类号: C07K5/06139 , A61K38/00 , C07D277/56 , C07D417/12 , C07D417/14 , C07K5/021 , C07K5/06034 , C07K5/06043 , C07K5/06052
摘要: The present invention provides one or more compounds of formula (I) for conjugation to small molecules, polymers, peptides, proteins, antibodies, antibody fragments etc.
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4.
公开(公告)号:US20180353548A1
公开(公告)日:2018-12-13
申请号:US15570316
申请日:2016-04-28
IPC分类号: A61K35/28 , C07K5/062 , C12N5/0775 , A61P29/00 , A61P43/00
CPC分类号: A61K35/28 , A61K9/0019 , A61K35/12 , A61P29/00 , A61P43/00 , C07K5/06034 , C12N5/0663 , C12N2500/95
摘要: Preparations comprising an enriched population of extracellular vesicles (nEVs) having a negatively charged surface, and that are CD81+ and CD9−, are provided. Improved processes and methods for producing an enriched population of nEVs from non-murine cells, especially human origin cells and/or tissues, are disclosed. Therapeutic methods for using the preparations, including for reducing brain inflammation and treatment of various pathologies associated with brain inflammation, such as by intravenous or intranasal administration, are also described. Methods and preparations for reducing brain inflammation associated with traumatic brain injury (TBI) are also disclosed. A method for treating a patient having suffered a mild traumatic injury (mTMI), or concussion, such as a sports-related head injury, is also disclosed. The nEVs are also demonstrated to reduce the expression level of IL-Iβ in brain tissue of an animal having had traumatic brain injury. Methods for improving cognitive function and performance in animals after a traumatic brain injury is also demonstrated using the preparations of nEVs disclosed herein.
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公开(公告)号:US20180327449A1
公开(公告)日:2018-11-15
申请号:US15974855
申请日:2018-05-09
IPC分类号: C07K5/062 , C07K5/083 , C07K5/08 , C07D207/16 , C07D307/02 , C07D477/02 , C07D477/20 , C07K5/06 , C07K5/02 , A61K38/00
CPC分类号: C07K5/06034 , A61K38/00 , C07D207/16 , C07D307/02 , C07D477/02 , C07D477/20 , C07K5/0202 , C07K5/0205 , C07K5/06 , C07K5/06008 , C07K5/06191 , C07K5/08 , C07K5/0808 , Y02A50/385 , Y02A50/387 , Y02A50/389 , Y02A50/475
摘要: This invention describes an ICE inhibitor prodrug (I) having good bioavailability. Compound I is useful for treating IL-1 mediated diseases such as rheumatoid arthritis, inflammatory bowel disease, Crohn's disease, ulcerative colitis, inflammatory peritonitis, septic shock, pancreatitis, traumatic brain injury, organ transplant rejection, osteoarthritis, asthma, psoriasis, Alzheimer's disease, myocardial infarction, congestive heart failure, Huntington's disease, atherosclerosis, atopic dermatitis, leukemias and related disorders, myelodysplastic syndrome, uveitis or multiple myeloma.
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公开(公告)号:US20180303741A1
公开(公告)日:2018-10-25
申请号:US16022809
申请日:2018-06-29
发明人: Ruey J. YU , Eugene J. VAN SCOTT
CPC分类号: A61K8/64 , A61K8/671 , A61K9/0014 , A61K31/07 , A61K38/05 , A61K2800/10 , A61K2800/92 , A61Q5/00 , A61Q19/00 , A61Q19/007 , A61Q19/008 , A61Q19/02 , A61Q19/06 , A61Q19/08 , C07K5/0202 , C07K5/0205 , C07K5/0207 , C07K5/06026 , C07K5/06034 , C07K5/06043 , C07K5/06052 , C07K5/0606 , C07K5/06069 , C07K5/06078 , C07K5/06113 , C07K5/06147 , C07K5/06156 , C07K5/06165 , C07K5/06191 , Y02A50/463
摘要: Methods of treating aging related skin changes and of increasing skin thickness with topical administration of N-acyldipeptide derivatives and retinol are described. Combinations of retinol and N-acyldipeptide derivatives, are therapeutically effective for increasing skin thickness, and for treating extrinsic and intrinsic aging and aging related skin changes, such as fine lines, wrinkles, photoaging, hyperpigmentation, laxity, age spots, lentigines, mottled skin, and cellulite.
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公开(公告)号:US20180259535A1
公开(公告)日:2018-09-13
申请号:US15974923
申请日:2018-05-09
申请人: Warp Drive Bio, Inc.
发明人: Gregory L. VERDINE , M. James NICHOLS , Sharon A. TOWNSON , Uddhav Kumar SHIGDEL , Seung-Joo LEE , Dylan T. STILES , Neville J. ANTHONY
IPC分类号: G01N33/68 , C07K5/083 , C07K1/13 , C07K5/02 , C07K7/64 , C12Q1/533 , C07K1/08 , C07K5/062 , G01N33/566
CPC分类号: G01N33/6845 , C07K1/086 , C07K1/13 , C07K5/0215 , C07K5/06034 , C07K5/0808 , C07K7/64 , C07K7/645 , C12Q1/533 , G01N33/566 , G01N2333/82 , G01N2333/90209 , G01N2410/08 , G01N2500/02
摘要: The present disclosure provides methods and reagents useful for analyzing protein-protein interfaces such as interfaces between a presenter protein (e.g., a member of the FKBP family, a member of the cyclophilin family, or PIN1) and a target protein. In some embodiments, the target and/or presenter proteins are intracellular proteins. In some embodiments, the target and/or presenter proteins are mammalian proteins.
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公开(公告)号:US20180252726A1
公开(公告)日:2018-09-06
申请号:US15974921
申请日:2018-05-09
申请人: Warp Drive Bio, Inc.
发明人: Gregory L. VERDINE , M. James NICHOLS , Sharon A. TOWNSON , Uddhav Kumar SHIGDEL , Seung-Joo LEE , Dylan T. STILES , Neville J. ANTHONY
IPC分类号: G01N33/68 , C07K5/083 , C07K1/13 , C07K5/02 , C07K7/64 , C12Q1/533 , C07K1/08 , C07K5/062 , G01N33/566
CPC分类号: G01N33/6845 , C07K1/086 , C07K1/13 , C07K5/0215 , C07K5/06034 , C07K5/0808 , C07K7/64 , C07K7/645 , C12Q1/533 , G01N33/566 , G01N2333/82 , G01N2333/90209 , G01N2410/08 , G01N2500/02
摘要: The present disclosure provides methods and reagents useful for analyzing protein-protein interfaces such as interfaces between a presenter protein (e.g., a member of the FKBP family, a member of the cyclophilin family, or PIN1) and a target protein. In some embodiments, the target and/or presenter proteins are intracellular proteins. In some embodiments, the target and/or presenter proteins are mammalian proteins.
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9.
公开(公告)号:US20180228772A1
公开(公告)日:2018-08-16
申请号:US15949335
申请日:2018-04-10
申请人: Allergan, Inc.
IPC分类号: A61K31/417 , C07D233/64 , C07C317/50 , C07C275/30 , C07C323/44 , C07C317/42 , A61K31/198 , A61K31/17 , C07K5/072 , C07K5/062 , C07K5/078 , A61K31/216 , A61K31/197 , A61K31/4045 , C07C323/60 , C07D209/20
CPC分类号: A61K31/417 , A61K31/17 , A61K31/197 , A61K31/198 , A61K31/216 , A61K31/4045 , C07C275/30 , C07C317/42 , C07C317/50 , C07C323/44 , C07C323/60 , C07D209/20 , C07D233/64 , C07K5/06017 , C07K5/06034 , C07K5/06052 , C07K5/0606 , C07K5/06113 , C07K5/06147 , C07K5/06156 , Y02A50/401
摘要: The present invention relates to novel amide derivatives of N-urea substituted amino acids, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.
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公开(公告)号:US09988423B2
公开(公告)日:2018-06-05
申请号:US14380615
申请日:2013-02-22
发明人: Charlotte Hauser , Archana Mishra
IPC分类号: A61K38/00 , A61P17/00 , A61K38/08 , A61K38/06 , A61K38/07 , C08L89/00 , C08L91/00 , C09D189/00 , C09D191/00 , C09J189/00 , C09J191/00 , H01B1/00 , H01B1/12 , A23L1/05 , A23L1/06 , C07K7/06 , A61K8/64 , C07K5/083 , C07K5/062 , A61K9/06 , A61K47/34 , A61K8/04 , A61Q19/00 , A61K9/107 , A61K45/06 , H01L51/00
CPC分类号: C07K7/06 , A61K8/042 , A61K8/64 , A61K9/06 , A61K9/107 , A61K38/06 , A61K38/08 , A61K45/06 , A61K47/34 , A61K2800/10 , A61K2800/48 , A61Q19/00 , C07K5/06034 , C07K5/0808 , H01L51/0093
摘要: The present invention relates to organogels and emulsions based on ultrasmall self-assembling peptides. It further relates to methods for producing such organogels and emulsions as well as to the use of the organogels and emulsions in biological and non-biological applications.
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