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1. 发明授权

US11560352B2 P62-ZZ small molecule modulators 有权
公开(公告)号：US11560352B2
公开(公告)日：2023-01-24
申请号：US16942548
申请日：2020-07-29
申请人： University of Pittsburgh—Of the Commonwealth System of Higher Education
发明人： Xiangqun Xie
IPC分类号： C07C217/58 , A61K31/137 , A61K45/06 , A61P35/00
摘要： A compound, or a pharmaceutically acceptable salt thereof, having a formula I of: wherein Ar is an arylene or heteroarylene; R1 has a structure of: wherein W is an alkanediyl, alkenediyl, a carbonyl, or a combination thereof; X is —NR5—, wherein R5 is H or an alkyl, or —O—; and Y is optionally-substituted cycloalkyl, optionally-substituted cycloalkyl-substituted alkyl, optionally-substituted heterocycloalkyl, or optionally-substituted heterocycloalkyl-substituted alkyl; each R2 is the same or different and has a structure of: wherein Z is —NR6—, wherein R6 is H or an alkyl, —O—, —S—, or —CH2—; Z1 is (—CH2-)m wherein m is 0 to 5, or an alkenediyl having 2 to 6 carbon atoms; Cy is a 3-8-membered cycloalkyl, heterocycloalkyl, aryl or heteroaryl ring; and each R4 is the same or different and is selected from hydroxy, halogen, substituted or unsubstituted alkoxy, substituted or unsubstituted alkyl, or amino; and c is 0 to 5; and each R3 is the same or different and is selected from hydroxy, halogen, substituted or unsubstituted alkoxy, substituted or unsubstituted alkyl, amino, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or a nitro, wherein a is 2 to 5, and b is 0 to 3.

2. 发明申请

US20220354949A1 NOVEL COMPOUNDS 有权
公开(公告)号：US20220354949A1
公开(公告)日：2022-11-10
申请号：US17270665
申请日：2019-08-23
申请人： XENIOPRO GmbH
发明人： Viktoria REINMÜLLER , Roman MARTY , Olivier WAGNIÈRES , Jean-Baptiste GUALTIEROTTI , Verena KÜPPERS
IPC分类号： A61K39/39 , C07C311/51 , C07D213/89 , C07C261/04 , C07C259/10 , C07C325/02 , C07D405/04 , C07C217/58 , C07C239/12 , C07C255/43 , C07D309/06 , C07D211/22 , C07D295/092 , C07D453/02 , C07D205/04 , C07D491/107 , C07D401/12 , C07D405/12 , C07D519/00 , C07D407/12 , C07D331/04 , C07D409/12 , C07D211/28 , C07D305/04 , C07C69/78 , C07C47/198 , C07D213/80 , C07D213/643 , C07D237/04 , C07D239/47 , C07D239/52
摘要： The present invention comprises novel aromatic molecules, which can be used in the treatment of pathological conditions, such as cancer, skin diseases, muscle disorders, and immune system-related disorders such as disorders of the haematopoietic system including the haematologic system in human and veterinary medicine.

3. 发明授权

US11479529B2 Compounds with antimicrobial activity 有权
公开(公告)号：US11479529B2
公开(公告)日：2022-10-25
申请号：US16959142
申请日：2019-01-08
申请人： The Hong Kong Polytechnic University , The Chinese University of Hong Kong
发明人： Cong Ma , Xiao Yang
IPC分类号： C07C251/86 , A61P31/04 , C07C215/50 , C07C217/58 , C07C251/24 , C07C255/53 , C07C255/58 , C07C255/59 , C07C255/61 , C07C311/39 , C07C311/44 , C07D257/04 , C07D231/20 , C07D231/42 , C07D249/12 , C07D307/90 , C07D403/12
摘要： This invention relates to compounds of formula 1, 2 or 3 a pharmaceutically acceptable salt, or solvate thereof, wherein X1, Y, R1, R2, R3, R4, and R5 are as defined herein. The compounds are antimicrobial agents that may be used to treat various bacterial and protozoal infections and disorders related to such infections. The invention also relates to pharmaceutical compositions containing the compounds and to methods of treating bacterial and protozoal infections by administering the compounds of formula 1, 2 or 3.

4. 发明申请

US20220064151A1 ACTIVATORS OF CLASS I HISTONE DEACETYLASES (HDACS) AND USES THEREOF 有权
公开(公告)号：US20220064151A1
公开(公告)日：2022-03-03
申请号：US17397752
申请日：2021-08-09
申请人： Massachusetts Institute of Technology , The General Hospital Corporation d/b/a Massachusetts General Hospital
发明人： Li-Huei Tsai , Ling Pan , Stephen J. Haggarty , Debasis Patnaik
IPC分类号： C07D405/12 , C07D307/52 , C07D411/12 , C07D307/40 , C07C217/58 , C07D487/04 , C07C219/28 , C07D409/12
摘要： The present invention provides compounds of Formulae (A), (B), (C), and (D), pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, and prodrugs thereof, pharmaceutical compositions thereof, and kits thereof. The present invention further provides methods of using the compounds to treat or prevent neurological disorders, including Alzheimer's disease, Parkinson's disease, Huntington's disease, ALS (amyotrophic lateral sclerosis), traumatic brain injury, ischemic brain injury, stroke, frontal temporal dementia, Pick's disease, corticobasal degeneration, supra cerebral palsy, prion diseases (e.g., Creutzfeldt-Jakob disease, Gerstmann-Straussler-Scheinker syndrome, Fatal Familial Insomnia, and Kuru), Nieman Pick type C, spinal cerebellar ataxia, spinal muscular dystrophy, ataxia telangiectasia, hippocampal sclerosis, Cockayne syndrome, Werner syndrome, xeroderma pigmentosaum, and Bloom syndrome. In one aspect, the methods include administering to a subject in need of treatment for a neurological disorder a therapeutically effective amount of DAC-001, DAC-002, DAC-003, DAC-009, or DAC-012, or a compound of Formula (A), (B), (C), or (D).

5. 发明授权

US11174223B2 Compositions, methods, and systems for the synthesis and use of imaging agents 有权
公开(公告)号：US11174223B2
公开(公告)日：2021-11-16
申请号：US15593540
申请日：2017-05-12
申请人： Lantheus Medical Imaging, Inc.
发明人： Ajay Purohit , Pedro Benites , Heike S. Radeke , Joel Lazewatsky , L. Veronica Lee
IPC分类号： A61K51/00 , A61M36/14 , C07C303/30 , A61K51/04 , C07B59/00 , C07C53/06 , C07C217/58 , C07C255/54 , C07C279/10 , C07C279/24 , C07C309/65 , C07C309/66 , C07C309/73 , C07C277/08 , C07C53/10 , C07C53/18 , C07C63/08 , C07C213/02 , C07C303/28 , C07C309/04 , C07C309/30 , C07C277/00
摘要： The present invention generally relates to novel synthetic methods, systems, kits, salts, and precursors useful in medical imaging. In some embodiments, the present invention provides compositions comprising an imaging agent precursor, which may be formed using the synthetic methods described herein. An imaging agent may be converted to an imaging agent using the methods described herein. In some cases, the imaging agent is enriched in 18F. In some cases, an imaging agent including salt forms (e.g., ascorbate salt) may be used to image an area of interest in a subject, including, but not limited to, the heart, cardiovascular system, cardiac vessels, brain, and other organs.

6. 发明申请

US20210309641A1 AMIDINES AND AMIDINE ANALOGS FOR THE TREATMENT OF BACTERIAL INFECTIONS AND POTENTIATION ANTIBIOTICS 有权
公开(公告)号：US20210309641A1
公开(公告)日：2021-10-07
申请号：US17251658
申请日：2019-06-13
申请人： GEORGIA STATE UNIVERSITY RESEARCH FOUNDATION, INC.
发明人： Binghe Wang , David W. Boykin , Manjusha Roy Choudhury , Arvind Kumar , Bingchen Yu , Mengyuan Zhu
IPC分类号： C07D403/12 , C07C217/58 , C07C257/18 , C07C321/28 , C07D409/04 , A61K45/06
摘要： Compounds and methods for the treatment of a bacterial infection or the potentiation of an antibiotic in treating a bacterial infection are described herein.

7. 发明申请

US20210052585A1 SUBSTITUTED 1,1'-BIPHENYL COMPOUNDS, ANALOGUES THEREOF, AND METHODS USING SAME 有权
公开(公告)号：US20210052585A1
公开(公告)日：2021-02-25
申请号：US16982842
申请日：2019-03-29
申请人： Arbutus Biopharma Corporation
发明人： Yingzhi Bi , Bruce D. Dorsey , Yi Fan , Christopher Brooks Moore , Duyan Nguyen
IPC分类号： A61K31/506 , A61K45/06 , C07D233/26 , C07D239/06 , C07C255/61 , C07D401/12 , C07D401/14 , C07D211/60 , C07C217/58 , A61K31/4164 , A61K31/505 , A61K31/277 , A61K31/4545 , A61K31/444 , A61K31/445 , A61K31/137
摘要： The present invention includes substituted 3,3′bis(phenoxymethyl)-1,1′-biphenyl compounds, analogues thereof, and compositions comprising the same, that can be used to treat or prevent hepatitis B virus (HBV) and/or hepatitis D virus (HDV) infections in a patient.

8. 发明申请

US20210017120A1 NITROBENZYL DERIVATIVES OF ANTI-CANCER AGENTS 有权
公开(公告)号：US20210017120A1
公开(公告)日：2021-01-21
申请号：US17036588
申请日：2020-09-29
申请人： OBI PHARMA, INC.
发明人： Jian-Xin Duan , Yeyu Cao , Xiaohong Cai , Hailong Jiao , Jing Yuan Ma , Mark Matteucci
IPC分类号： C07C217/58 , C07D405/12 , C07F9/6558 , A61K47/64 , C07D403/06 , A61K47/55 , A61P35/00 , C07D239/94 , C07D487/04 , C07D471/04 , C07C213/02 , C07D491/22 , C07H19/06
摘要： Provided herein are compounds of formula I: wherein the variables are defined herein, processes of making them, and methods of treating cancer comprising administering such compounds.

9. 发明授权

US10709719B2 Substituted bicyclic compounds 有权
公开(公告)号：US10709719B2
公开(公告)日：2020-07-14
申请号：US16188444
申请日：2018-11-13
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： Alaric J. Dyckman , T. G. Murali Dhar , Hai-Yun Xiao , John L. Gilmore , Michael G. Yang , Zili Xiao , David Marcoux
IPC分类号： A61K31/695 , C07F7/08 , A61K31/135 , C07D215/14 , C07D241/04 , C07C323/29 , C07C251/38 , C07C251/42 , C07C251/44 , C07D209/46 , C07D213/38 , C07C275/26 , C07C217/74 , C07C323/25 , C07C235/46 , C07F9/54 , C07F9/572 , C07F9/09 , C07C215/42 , C07C217/52 , C07C217/58 , C07C219/24 , C07C233/41 , C07C233/65 , C07C251/50 , C07C251/52 , C07C251/54 , C07C271/34 , C07C317/28 , C07C317/32 , C07C321/16 , C07C321/22 , C07C321/28 , C07D213/32 , C07D213/69 , C07D213/70 , C07D215/12 , C07D217/24 , C07D231/12 , C07D231/20 , C07D239/26 , C07D241/12 , C07D277/24 , C07D305/08 , C07D309/06 , C07D309/12 , C07D311/58 , C07D311/76 , C07D319/20 , C07D333/16 , C07F9/117 , C07F9/62 , C07F9/6503 , C07F9/6509 , C07F9/655 , C07F9/6553 , A61K31/137 , A61K31/15 , A61K31/165 , A61K31/166 , A61K31/17 , A61K31/222 , A61K31/24 , A61K31/27 , A61K31/337 , A61K31/351 , A61K31/352 , A61K31/381 , A61K31/415 , A61K31/4174 , A61K31/426 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/47 , A61K31/4965 , A61K31/505 , A61K31/661
摘要： Disclosed are compounds of Formulas (I), (II), (III), (IV), and (V): and/or a salt thereof, wherein R1 is —OH or —OP(O)(OH)2, and X1, X2, X3, R2, R2a, Ra, Rb, and Rc are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.

10. 发明授权

US10577308B2 Sodium channel modulators 有权
公开(公告)号：US10577308B2
公开(公告)日：2020-03-03
申请号：US15561674
申请日：2016-03-24
申请人： The Florey Institute of Neuroscience and Mental Health , The University of Melbourne
发明人： Spencer John Williams , Bevyn Jarrott
IPC分类号： C07D213/36 , C07C217/18 , C07D231/56 , C07D239/26 , C07D403/12 , C07D401/14 , C07D271/06 , C07C255/58 , C07C217/58 , C07C233/43 , C07C311/37 , C07C311/16
摘要： The present disclosure relates generally to compounds having activity as voltage-gated sodium channel blockers and their use in the field of therapeutic treatment, including the therapy or management of conditions associated with excessive, unwanted, inadequate or otherwise undesirable sodium ion passage through cellular membranes via voltage-gated sodium channels. In some embodiments, the disclosure relates to aryloxy-substituted amines for use as sodium channel blockers or modulators. Methods for their manufacture and compositions containing the compounds are also disclosed.

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