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1. 发明申请

US20190185439A1 RADIOFLUORINATED CARBOXIMIDAMIDES AS IDO TARGETING PET TRACER FOR CANCER IMAGING 审中-公开
公开(公告)号：US20190185439A1
公开(公告)日：2019-06-20
申请号：US16327372
申请日：2017-08-24
申请人： H. LEE MOFFITT CANCER CENTER & RESEARCH INSTITUTE, INC.
发明人： Haibin TIAN , Robert GILLIES
IPC分类号： C07D271/08 , C07B59/00
CPC分类号： C07D271/08 , A61K45/06 , A61K51/0453 , A61K2123/00 , C07B59/002 , C07B2200/05 , C07D271/02 , C07D273/02
摘要： Radiofluorinated carboximidamides are disclosed as selective IDO enzyme radioligands and generate specific binding in accordance with IDO expression in vitro. MicroPET experiments indicate [18F]IDO49 specifically accumulate in IDO-expressing tumors which confirmed by Western blot and IHC analysis supported. Using Hela tumor bearing models with IFN-γ treatment confirmed that [18F]IDO49 accumulation in the IFN-γ treatment tumor mouse. These results can have implications that [18F]IDO49 has substantial potential as an imaging agent that targets IDO in tumors.

2. 发明申请

US20170066753A1 OXADIAZINE COMPOUNDS AND METHODS OF USE THEREOF 有权
公开(公告)号：US20170066753A1
公开(公告)日：2017-03-09
申请号：US15178626
申请日：2016-06-10
申请人： FORUM Pharmaceuticals Inc.
发明人： Raksha Acharya , Duane A. Burnett , Matthew Gregory Bursavich , Andrew Simon Cook , Bryce Alden Harrison , Andrew J. McRiner
IPC分类号： C07D413/14 , C07D417/14 , C07D471/04 , C07D413/04
CPC分类号： C07D413/14 , A61K31/535 , C07D247/02 , C07D271/02 , C07D273/02 , C07D273/04 , C07D413/04 , C07D417/14 , C07D471/04
摘要： The present disclosure relates to oxadiazine compounds, pharmaceutical compositions comprising an effective amount of an oxadiazine compound and methods for using an oxadiazine compound in the treatment of a neurodegenerative disease, comprising administering to a subject in need thereof an effective amount of an oxadiazine compound.

3. 发明授权

US08530646B2 Oxazolidinone derivative having 7-membered hetero ring 失效
标题翻译：具有7元杂环的恶唑烷酮衍生物
公开(公告)号：US08530646B2
公开(公告)日：2013-09-10
申请号：US12733954
申请日：2008-10-01
申请人： Hideyuki Suzuki , Iwao Utsunomiya , Koichi Shudo , Tsutomu Iwaki , Tatsuro Yasukata
发明人： Hideyuki Suzuki , Iwao Utsunomiya , Koichi Shudo , Tsutomu Iwaki , Tatsuro Yasukata
IPC分类号： C07D273/06 , C07D255/00 , C07D255/02
CPC分类号： C07D413/14 , C07D271/02 , C07D413/10 , C07D471/14 , C07D487/04 , Y02P20/55
摘要： The present invention provides a novel oxazolidinone derivative of the formula (I): wherein Rings A and B are defined as in the specification; X1is a single bond, or a heteroatom-containing group selected from the group consisting of —O—, —S—, —NR2—, —CO—, —CS—, —CONR3—, —NR4CO—, —SONR5—, and NR6SO2—, wherein R2, R3, R4, R5, and R6 are independently hydrogen or lower alkyl, or lower alkylene or lower alkenylene each optionally interrupted by said heteroatom containing group; and R1 is hydrogen, or an organic residue which is able to bind to the 5-position of the oxazolidinone ring in oxazolidinone antimicrobial agents, pharmaceutically acceptable salts and solvates thereof which are useful as an antibacterial agent.
摘要翻译：本发明提供式（I）的新型恶唑烷酮衍生物：其中环A和B如说明书中所定义; X1是单键或选自-O - ， - S - ， - NR 2 - ， - CO - ， - CS - ， - CONR 3 - ， - NR 4 CO-，-SONR 5 - 和 - NR 6 SO 2 - ，其中R 2，R 3，R 4，R 5和R 6独立地为氢或低级烷基，或低级亚烷基或低级亚烯基，各自任选被所述含杂原子基团间隔; R 1为氢，或可用于作为抗菌剂使用的恶唑烷酮抗微生物剂，其药学上可接受的盐和溶剂合物中的恶唑烷酮环的5位的有机残基。

4. 发明授权

US5175224A Polyimide from bis-maleimide having azole ring 失效
标题翻译：来自具有AZOLE环的双 - 马来酰亚胺的聚酰亚胺
公开(公告)号：US5175224A
公开(公告)日：1992-12-29
申请号：US573035
申请日：1990-08-22
申请人： Heinz Horacek
发明人： Heinz Horacek
IPC分类号： C07D249/02 , C07D249/12 , C07D263/46 , C07D271/02 , C07D275/02 , C07D277/12 , C07D277/20 , C07D277/32 , C07D277/34 , C07D277/36 , C07D285/08 , C07D285/12 , C07D285/125 , C07D285/13 , C07D403/12 , C07D403/14 , C07D417/12 , C07D417/14 , C08G73/10 , C08G73/12 , C08J5/24 , H05K1/03
CPC分类号： C07D277/32 , C07D249/02 , C07D249/12 , C07D263/46 , C07D271/02 , C07D277/36 , C07D285/125 , C07D403/14 , C07D417/14 , C08G73/124 , C08G73/125 , H05K1/0346
摘要： A diamine or bismaleimide of the general formula I ##STR1## in which R.sub.1 and R.sub.2 denote an H atom or together denote the group --OC--CH.dbd.CH--CO--, Y.sub.1 and Y.sub.2 independently of one another deonte O or S and Het denotes a thiazole, a thiadiazole or a 1-methyltriazole ring. The diamines and bismaleimides are used for the preparation of polyimides which are if appropriate reinforced with fibers and if appropriate incompletely hardened.
摘要翻译： PCT No.PCT / EP89 / 00120 Sec。 371日期1990年8月22日 102（e）日期1990年8月22日PCT提交1989年2月9日PCT公布。出版物WO89 / 08107 日本1989年9月8日。一种通式I的二胺或双马来酰亚胺，其中R 1和R 2表示H原子，或一起表示基团-OC-CH = CH-CO-，Y 1和Y 2独立地为一个另一个脱醛O或S和Het表示噻唑，噻二唑或1-甲基三唑环。二胺和双马来酰亚胺用于制备聚酰亚胺，其如果适用于纤维增强并且如果适当的话，不完全硬化。

5. 发明授权

US09802927B2 Oxadiazine compounds and methods of use thereof 有权
公开(公告)号：US09802927B2
公开(公告)日：2017-10-31
申请号：US15178626
申请日：2016-06-10
申请人： Denali Therapeutics, Inc.
发明人： Raksha Acharya , Duane A. Burnett , Matthew Gregory Bursavich , Andrew Simon Cook , Bryce Alden Harrison , Andrew J. McRiner
IPC分类号： C07D498/04 , C07D413/14 , A61K31/535 , C07D247/02 , C07D271/02 , C07D273/02 , C07D273/04 , C07D413/04 , C07D417/14 , C07D471/04
CPC分类号： C07D413/14 , A61K31/535 , C07D247/02 , C07D271/02 , C07D273/02 , C07D273/04 , C07D413/04 , C07D417/14 , C07D471/04
摘要： The present disclosure relates to oxadiazine compounds, pharmaceutical compositions comprising an effective amount of an oxadiazine compound and methods for using an oxadiazine compound in the treatment of a neurodegenerative disease, comprising administering to a subject in need thereof an effective amount of an oxadiazine compound.

6. 发明申请

US20170029388A1 Treatment of Neurodegenerative Diseases with Asparagine Endopeptidase (AEP) Inhibitors and Compositions Related Thereto 审中-公开
标题翻译：用天门冬酰胺内肽酶（AEP）抑制剂和组合物治疗神经退行性疾病
公开(公告)号：US20170029388A1
公开(公告)日：2017-02-02
申请号：US15303458
申请日：2015-04-08
申请人： INTERCONTINENTAL GREAT BRANDS LLC
发明人： Keqiang Ye , Haian Fu , Yuhong Du
IPC分类号： C07D271/12
CPC分类号： C07D271/12 , A61K9/20 , A61K9/48 , A61K31/4015 , A61K31/426 , A61K31/433 , A61K31/47 , A61K31/496 , A61K31/519 , A61K31/522 , A61K31/5377 , C07D271/02 , C07D471/04 , C07D473/04 , Y02A50/395
摘要： This disclosure relates to asparagine endopeptidase inhibitors and compositions and uses related thereto. In certain embodiments, the asparagine endopeptidase inhibitors are useful for treating or preventing neurodegenerative diseases and cognitive disorders such as Alzheimer's Disease. In certain embodiments, the disclosure relates to pharmaceutical compositions comprising an asparagine endopeptidase inhibitor and a pharmaceutically acceptable excipient. In certain embodiments, the disclosure relates to methods of treating or preventing a neurodegenerative disease comprising administering an effective amount of pharmaceutical composition a asparagine endopeptidase inhibitor disclosed herein to a subject in need thereof.
摘要翻译：本公开涉及天冬酰胺内肽酶抑制剂及其组合物和用途。在某些实施方案中，天冬酰胺内肽酶抑制剂可用于治疗或预防神经变性疾病和认知障碍如阿尔茨海默病。在某些实施方案中，本公开涉及包含天冬酰胺内肽酶抑制剂和药学上可接受的赋形剂的药物组合物。在某些实施方案中，本公开涉及治疗或预防神经变性疾病的方法，包括向有需要的受试者施用有效量的本文公开的天冬酰胺内肽酶抑制剂的药物组合物。

7. 发明申请

US20160264566A1 ANTI-ALPHAVBETA1 INTEGRIN INHIBITORS AND METHODS OF USE 审中-公开
标题翻译：抗ALPHAVBETA1 INTEGRIN抑制剂及其使用方法
公开(公告)号：US20160264566A1
公开(公告)日：2016-09-15
申请号：US15067124
申请日：2016-03-10
申请人： The Regents of the University of California
发明人： William F. DeGrado , Dean Sheppard , Hyunil Jo , Nilgun Isik Reed , Youzhi Tang , Joel McIntosh
IPC分类号： C07D417/12 , C07D249/06 , C07C279/14 , C07D471/04 , C07D233/50 , C07D217/24 , C07D263/32 , C07D277/30 , C07D401/12 , C07D239/14 , C07D413/12 , C07D403/12 , C07D271/02 , C07D285/04 , G01N33/68 , C07D213/74
CPC分类号： C07D417/12 , C07C279/14 , C07D213/74 , C07D217/24 , C07D233/50 , C07D239/14 , C07D249/06 , C07D263/32 , C07D271/02 , C07D277/30 , C07D285/04 , C07D401/12 , C07D403/12 , C07D413/12 , C07D471/04 , G01N33/573 , G01N33/6863 , G01N2333/7055
摘要： Provided herein, inter alia, are methods and compositions for inhibiting αvβ1 integrin and for treating fibrosis.
摘要翻译：本文提供了用于抑制αvβ1整联蛋白和治疗纤维化的方法和组合物。

8. 发明申请

US20100256355A1 OXAZOLIDINONE DERIVATIVE HAVING 7-MEMBERED HETERO RING 失效
标题翻译：具有7层杂环的氧杂环丁酮衍生物
公开(公告)号：US20100256355A1
公开(公告)日：2010-10-07
申请号：US12733954
申请日：2008-10-01
申请人： Hideyuki Suzuki , Iwao Utsunomiya , Koichi Shudo , Tsutomu Iwaki , Tatsuro Yasukata
发明人： Hideyuki Suzuki , Iwao Utsunomiya , Koichi Shudo , Tsutomu Iwaki , Tatsuro Yasukata
IPC分类号： C07D487/04 , C07D255/02 , C07D487/14
CPC分类号： C07D413/14 , C07D271/02 , C07D413/10 , C07D471/14 , C07D487/04 , Y02P20/55
摘要： The present invention provides a novel oxazolidinone derivative of the formula (I): wherein Ring A is (A-1) a 7-membered monocyclic heterocycle containing three N atoms; (A-2) a 7-membered monocyclic heterocycle containing two N atoms and one O atom; or (A-3) a 7-membered monocyclic heterocycle containing two N atoms and one S atom, SO or SO2, wherein said monocyclic heterocycle is optionally substituted, optionally unsaturated and optionally fused with another ring; X1 is a single bond, or a heteroatom-containing group selected from the group consisting of —O—, —S—, —NR2—, —CO—, —CS—, —CONR3—, —NR4CO—, —SO2NR5—, and —NR6SO2—, wherein R2, R3, R4, R5 and R6 are independently hydrogen or lower alkyl, or lower alkylene or lower alkenylene each optionally interrupted by said heteroatom-containing group; Ring B is optionally substituted carbocycle or optionally substituted heterocycle; and R1 is hydrogen, or an organic residue which is able to bind to the 5-position of the oxazolidinone ring in oxazolidinone antimicrobial agents, pharmaceutically acceptable salts and solvates thereof which are useful as an antibacterial agent.
摘要翻译：本发明提供式（I）的新型恶唑烷酮衍生物：其中环A为（A-1）含有三个N原子的7-元单环杂环; （A-2）含有两个N原子和一个O原子的7-元单环杂环; 或（A-3）含有两个N原子和一个S原子，SO或SO 2的7-元单环杂环，其中所述单环杂环任选被取代，任选地不饱和且任选地与另一个环稠合; X 1为单键或选自-O - ， - S - ， - NR 2 - ， - CO - ， - CS - ， - CONR 3 - ， - NR 4 CO - ， - SO 2 NR 5 - 和-NR 6 SO 2 - ，其中R 2，R 3，R 4，R 5和R 6独立地为氢或低级烷基，或低级亚烷基或低级亚烯基，各自任选被所述含杂原子基团中断; 环B是任选取代的碳环或任选取代的杂环; R 1为氢，或可用于作为抗菌剂使用的恶唑烷酮抗微生物剂，其药学上可接受的盐和溶剂合物中的恶唑烷酮环的5位的有机残基。

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