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1. 发明申请

US20210137938A1 NUPR1 INHIBITION FOR TREATING CANCER 有权
公开(公告)号：US20210137938A1
公开(公告)日：2021-05-13
申请号：US17059297
申请日：2019-05-31
申请人： INSTITUT NATIONAL DE SANTE ET DE LA RECHERCHE MEDICALE (INSERM) , FUNDACION AGENCIA ARAGONESA PARA LA INVESTIGACION Y EL DESARROLLO (ARAID) , MIGUEL HERNANDEZ UNIVERSITY OF ELCHE , FUNDACION INSTITUTO DE INVESTIGACION SANITARIA ARAGON , CHONGQING UNIVERSITY , INSTITUT JEAN PAOLI & IRENE CALMETES , UNIVERSITÉ D'AIX-MARSEILLE , UNIVERSITY OF ZARAGOZA , INSTITUTO ARAGONES DE CIENCIAS DE LA SALUD - ARAGON INSTITUTE OF HEALTH SCIENCES , CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS) , CONSIGLIO NAZIONALE DELLE RICERCHE- NATIONAL RESEARCH COUNCIL ITALY
发明人： Olga ABIAN FRANCO , Patricia SANTOFIMIA , Yi XIA , Jose Luis NEIRA , Bruno RIZZUTI , Adrian VELAZQUEZ CAMPOY , Ling PENG , Juan IOVANNA
IPC分类号： A61K31/5415 , A61K45/06 , C07D279/28 , C07D417/12 , A61P35/00
摘要： The present invention relates to the treatment of a tumor selected from the group consisting of pancreatic cancer, liver cancer, melanoma, colon cancer, glioblastoma, osteosarcoma, prostate cancer and breast cancer, more particularly pancreatic cancer. The inventors found a novel family compounds of formula (I) able to treat a variety of cancers by inhibiting NUPR1, a stress-inducible 82-amino-acid-long, intrinsically disordered member of the AT-hook family of chromatin proteins. Thus, the present invention relates to a compound of formula (I) for its use in the treatment of a tumor selected from the group consisting of pancreatic cancer, liver cancer, melanoma, colon cancer, glioblastoma, osteosarcoma, prostate cancer and breast cancer. In particular, the inventors tested compounds of formula (I) on four well characterized primary pancreatic cancer-derived cells 02.063 and LIPC (Basal subtype), Foic8b (derived from a liver metastasis) and HN14 (Classical subtype), as well as on other cellular lines derived from different tumors, i.e. U87 (glioblastoma), A375 and B16 (melanoma), U20S and SaOS (osteosarcoma), HT29, SK-CO-1 and LS174T (colon cancer), HepG2 (hepatocarcinoma), PC3 (prostate) and MDA-MB-231 (breast cancer). The compounds per se are also claimed.

2. 发明申请

US20210061837A1 PHENOTHIAZINE DERIVATIVES AND USES THEREOF 有权
公开(公告)号：US20210061837A1
公开(公告)日：2021-03-04
申请号：US16640482
申请日：2019-04-05
申请人： Camp4 Therapeutics Corporation
发明人： David A. Bumcrot , Alfica Sehgal , Donald L. Hertzog
IPC分类号： C07H7/06 , C07D279/28 , C07D417/06
摘要： The present invention provides phenothiazine compounds, processes for their preparation, pharmaceutical compositions comprising the compounds, and the use of the compounds or the compositions in the treatment of various diseases or conditions, for example ribosomal disorders and ribosomopathies, e.g. Diamond Blackfan anemia (DBA).

3. 发明申请

US20190233384A1 ANTI-INFECTIVE HETEROCYCLIC COMPOUNDS AND USES THEREOF 审中-公开
公开(公告)号：US20190233384A1
公开(公告)日：2019-08-01
申请号：US16312627
申请日：2017-06-22
申请人： Bioimics AB
发明人： Leif Kirsebom , Ram Shankar Upadhayaya , Raghava Reddy Kethiri , Anders Virtanen
IPC分类号： C07D279/28 , C07D279/20 , C07D265/38 , C07D241/46 , C07D417/14 , C07D417/04 , C07D417/06 , C07D417/12 , C07D413/12 , C07D513/04 , C07D513/06 , A61P31/04 , A61P31/10 , A61P33/00
CPC分类号： C07D279/28 , A61P31/04 , A61P31/10 , A61P33/00 , C07D241/46 , C07D265/38 , C07D279/20 , C07D413/12 , C07D417/04 , C07D417/06 , C07D417/12 , C07D417/14 , C07D513/04 , C07D513/06
摘要： The present invention relates to heterocyclic compounds of Formula I useful as anti-infective agents. The present invention further relates to a method of treating an infection by administering such compounds, and to pharmaceutical compositions comprising such compounds.

4. 发明申请

US20190106394A1 SUBSTITUTED BENZOXAZINE AND RELATED COMPOUNDS 审中-公开
公开(公告)号：US20190106394A1
公开(公告)日：2019-04-11
申请号：US16104840
申请日：2018-08-17
申请人： THE J. DAVID GLADSTONE INSTITUTES, A TESTAMENTARY TRUST ESTABLISHED UNDER THE WILL OF J. DAVID
发明人： Andrey S. Tsvetkov , Steven M. Finkbeiner , Michael A. Pleiss , Robert Greenhouse
IPC分类号： C07D265/36 , C07D498/04 , A61K9/08 , A61K9/10 , C07D279/28 , C07D279/16 , C07D209/08 , A61K9/02 , C07D413/06 , A61K9/48 , A61K9/20
摘要： The present invention relates to compounds including but not limited to of any one of formulas Ia, Ib, IIa, IIb, IIIa, IIIb, and IV to VI, VIIa, VIIb, VIIIa, VIIIb and VIIIc as described herein and their tautomers and/or pharmaceutically acceptable salts, compositions, and methods of uses thereof.

5. 发明授权

US10087151B2 Substituted benzoxazine and related compounds 有权
公开(公告)号：US10087151B2
公开(公告)日：2018-10-02
申请号：US15110082
申请日：2015-01-08
申请人： THE J. DAVID GLADSTONE INSTITUTES, A TESTAMENTARY TRUST ESTABLISHED UNDER THE WILL OF J. DAVID GLADSTONE
发明人： Andrey S. Tsvetkov , Steven M. Finkbeiner , Michael A. Pleiss , Robert Greenhouse
IPC分类号： C07D265/36 , C07D413/06 , C07D498/04 , C07D209/08 , C07D279/16 , C07D279/28 , A61K9/02 , A61K9/08 , A61K9/10 , A61K9/20 , A61K9/48
摘要： The present invention relates to compounds including but not limited to of any one of formulas Ia, Ib, IIa, IIb, IIIa, IIIb, and IV to VI, VIIa, VIIb, VIIIa, VIIIb and VIIIc as described herein and their tautomers and/or pharmaceutically acceptable salts, compositions, and methods of uses thereof.

6. 发明申请

US20180057471A1 Two-Electron Donating Phenothiazines and Use Thereof 审中-公开
公开(公告)号：US20180057471A1
公开(公告)日：2018-03-01
申请号：US15683679
申请日：2017-08-22
申请人： University of Kentucky Research Foundation
发明人： Susan A. Odom , Aman Preet Kaur , Matthew D. Casselman , N. Harsha Attanayake
IPC分类号： C07D279/28 , H01M8/18 , H01M8/1018 , C08G65/00
CPC分类号： C07D279/28 , C08G65/002 , C08G65/3348 , C08G2650/62 , C08G2650/64 , H01M8/1018 , H01M8/186 , H01M8/188
摘要： Compounds for use as electrolyte in a non-aqueous redox battery are provided, including an N-substituted phenothiazine compound according to the formula: R′ is alkyl and R is selected from alkyl, aryl, alkylaryl, alkoxyaryl, alkylcarboxyl, arylcarbonyl, haloalkyl, perfluoroalkyl, glycol, polyether, haloaryl, a negative electrolyte, a polymerizable unit, and a polymer.

7. 发明授权

US09370523B2 Method for diagnosing or prediagnosing a beta-amyloidopathy or an alpha-synucleopathy 有权
标题翻译：用于诊断或预诊断β-淀粉样变性或α-突触核蛋白病的方法
公开(公告)号：US09370523B2
公开(公告)日：2016-06-21
申请号：US14499918
申请日：2014-09-29
申请人： Immungenetics AG
发明人： Jens Pahnke
IPC分类号： G01N33/68 , A61K31/5415 , C07D279/24 , C07D417/06 , C07D417/14 , A61K31/495 , C07D279/28 , G01N33/48
CPC分类号： A61K31/5415 , A61K31/495 , C07D279/24 , C07D279/28 , C07D417/06 , C07D417/14 , G01N33/48 , G01N33/6896 , G01N2333/705 , G01N2800/2814 , G01N2800/2821 , G01N2800/2835
摘要： The invention relates to a method for the diagnosis or prediagnosis of a β-amyloidopathy or an α-synucleopathy accompanied by a cerebral protein deposit and a reduced activity of the cerebral ABCC1-transporter, or for determining the risk of a proband suffering from such an illness, the proband already having accumulated substances transported by the cerebral ABCC1 transporter.
摘要翻译：本发明涉及一种用于诊断或预诊和伴随脑蛋白沉积的α-突触核蛋白病和脑ABAC1转运蛋白活性降低的方法，或用于确定患有此类疾病的先证者的风险一种疾病，先证者已经积累了由大脑ABCC1转运蛋白运输的物质。

8. 发明授权

US07906643B2 Methylene blue-curcumin analog for the treatment of Alzheimer's Disease 有权
标题翻译：亚甲基蓝 - 姜黄素类似物用于治疗阿尔茨海默病
公开(公告)号：US07906643B2
公开(公告)日：2011-03-15
申请号：US12697503
申请日：2010-02-01
申请人： Thomas M DiMauro
发明人： Thomas M DiMauro
IPC分类号： C07D279/28 , A61K31/5415
CPC分类号： C07D279/28
摘要： A methylene blue-curcumin hybrid useful in treating Alzheimer's Disease.
摘要翻译：用于治疗阿尔茨海默氏病的亚甲基蓝 - 姜黄素杂合物。

9. 发明授权

US07723515B1 Methylene blue—curcumin analog for the treatment of alzheimer's disease 有权
标题翻译：亚甲基蓝 - 姜黄素类似物用于治疗阿尔茨海默病
公开(公告)号：US07723515B1
公开(公告)日：2010-05-25
申请号：US12359713
申请日：2009-01-26
申请人： Thomas M. DiMauro
发明人： Thomas M. DiMauro
IPC分类号： C07D279/28 , A61K31/5415
CPC分类号： C07D279/28
摘要： A methylene blue—curcumin hybrid useful in treating Alzheimer's Disease.
摘要翻译：用于治疗阿尔茨海默氏病的亚甲基蓝 - 姜黄素杂合物。

10. 发明授权

US6114392A Agmatine, and polyaminoguanidine-bound heterocyclic compounds for neurotrauma and neurodegenerative diseases 失效
标题翻译：苯胺和聚氨基胍结合的杂环化合物用于神经损伤和神经变性疾病
公开(公告)号：US6114392A
公开(公告)日：2000-09-05
申请号：US632835
申请日：1996-04-16
申请人： Gad M. Gilad , Varda H. Gilad
发明人： Gad M. Gilad , Varda H. Gilad
IPC分类号： A61K31/155 , C07D279/28 , A61K31/132 , A61K31/133 , A61K31/15
CPC分类号： C07D279/28 , A61K31/155
摘要： The invention relates to the use of agmatine, in the treatment of acute neurotrauma (such as stroke) and degenerative disorders of the central and peripheral nervous system (such as dementia).The invention further provides novel compounds of general formula I (which are quinuclidine derivatives), formula II (which are norbornane derivatives), formula III (which are adamantane derivatives), and formula IV (which are phenothiazine derivatives): ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are each independently hydrogen, hydroxy, substituted or unsubstituted C.sub.1-4 alkyl, substituted or unsubstituted C.sub.1-4 alkoxy, halogeno, amino, phenyl, or R.sub.4 NR.sub.5 ; R.sub.4 and R.sub.5 are each independently hydrogen, or (CH.sub.2)n--[NH(CH.sub.2)x]y--NHR.sub.6, or (CH.sub.2)n--[NH(CH.sub.2)x]y--NH--NHR.sub.6, or (CH.sub.2)n--[NH(CH.sub.2)x]y--(NR.sub.7 .dbd.)CNHR.sub.6, or (CH.sub.2)n--[NH(CH.sub.2)x]y--NH(NR.sub.7 .dbd.)CNHR.sub.6 wherein n is from 0-5, y is from 0-5 and each x is independently from 1-5; R.sub.6, and R.sub.7 are each independently hydrogen, hydroxy, substituted or unsubstituted C.sub.1-4 alkyl, substituted or unsubstituted C.sub.1-4 alkoxy, or halogeno; and pharmaceutically acceptable salts and optically active isomers thereof.
摘要翻译：本发明涉及用于治疗急性神经损伤（如中风）和中枢和周围神经系统退行性疾病（如痴呆）的用途。本发明还提供通式I（其为奎宁环衍生物），式II（其为降冰片烷衍生物），式III（其为金刚烷衍生物）和式IV（其为吩噻嗪衍生物）的新型化合物：其中R1，R2和 R 3各自独立地为氢，羟基，取代或未取代的C 1-4烷基，取代或未取代的C 1-4烷氧基，卤代，氨基，苯基或R 4 NR 5; R 4和R 5各自独立地为氢，或（CH 2）n - [NH（CH 2）x] y -NHR 6或（CH 2）n - [NH（CH 2）x] y -NH-NHR 6或（CH 2） [NH（CH 2）x] y - （NR 7 =）CNHR 6或（CH 2）n - [NH（CH 2）x] y -NH（NR 7 =）CNHR 6，其中n为0-5，y为0-5 并且每个x独立地为1-5; R 6和R 7各自独立地为氢，羟基，取代或未取代的C 1-4烷基，取代或未取代的C 1-4烷氧基或卤素; 及其药学上可接受的盐和旋光异构体。

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