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1. 发明授权

US09994573B2 Methods and reagents for radiolabeling 有权
公开(公告)号：US09994573B2
公开(公告)日：2018-06-12
申请号：US15107229
申请日：2014-12-23
申请人： Memorial Sloan-Kettering Cancer Center
发明人： Stefan O. Ochiana , NagaVaraKishore Pillarsetty , Tony Taldone , Gabriela Chiosis
IPC分类号： C07D473/34 , C07F7/22 , C07B59/00
CPC分类号： C07D473/34 , C07B59/002 , C07B2200/05 , C07F7/2208 , C07F7/2212
摘要： The present invention provides methods for radiolabeling compounds useful as Hsp90 inhibitors. The present invention also provides intermediates useful in such methods, and compositions of radiolabeled compounds. The present invention provides, among other things, novel methods for the synthesis of radiolabeled compounds. In certain embodiments, the present invention provides compounds of formula I.

2. 发明授权

US09878987B2 HSP70 modulators and methods for making and using the same 有权
公开(公告)号：US09878987B2
公开(公告)日：2018-01-30
申请号：US15310142
申请日：2015-05-13
申请人： Memorial Sloan Kettering Cancer Center
发明人： Gabriela Chiosis , Yanlong Kang , Hardik J. Patel , Maulik Patel , Stefan Ochiana , Anna Rodina , Tony Taldone , Liza Shrestha
IPC分类号： C07D239/46 , A61K31/506 , C07D405/12 , C07D401/12 , C07D403/04 , C07D417/12 , C07D413/12 , C07D407/12 , A61K31/5377 , A61K45/06
CPC分类号： C07D239/46 , A61K31/506 , A61K31/5377 , A61K45/06 , C07D239/42 , C07D401/12 , C07D403/04 , C07D405/12 , C07D407/12 , C07D413/12 , C07D417/12
摘要： The present invention provides compounds I and II and compositions thereof for use in the modulation of Hsp70. In some embodiments, the present invention provides a method for inhibiting Hsp70 activity. In some embodiments, the present invention provides a method of treating a subject suffering from or susceptible to a disease, disorder, or condition responsive to Hsp70 inhibition comprising administering to the subject a therapeutically effective amount of a provided compound. In some embodiments, the present invention provides a method for treating or preventing cancer in a subject suffering therefrom, comprising administering to a patient in need thereof a therapeutically effective amount of a provided compound.

3. 发明申请

US20140227183A1 SMALL-MOLECULE HSP90 INHIBITORS 有权
标题翻译：小分子HSP90抑制剂
公开(公告)号：US20140227183A1
公开(公告)日：2014-08-14
申请号：US14256510
申请日：2014-04-18
申请人： MEMORIAL SLOAN KETTERING CANCER CENTER
发明人： Gabriela Chiosis , Huazhong He , Laura Llauger-Bufi , Joungnam Kim , Steve M. Larson , Peter Smith-Jones
IPC分类号： C07D473/34 , C07D491/056 , G01N33/60 , A61K51/04
CPC分类号： C07D473/34 , A61K51/0459 , C07D491/056 , G01N33/60
摘要： Hsp90 inhibitors having are provided having the formula: (I) with a 2′,4′,5′-substitution pattern on the right-side aryl moiety. X1 represents two substituents, which may be the same or different, disposed in the 4′ and 5′ positions on the aryl group, wherein X1 is selected from halogen, alkyl, alkoxy, halogenated alkoxy, hydroxyalkyl, pyrollyl, optionally substituted aryloxy, alkylamino, dialkylamino, carbamyl, amido, alkylamido dialkylamido, acylamino, alkylsulfonylamido, trihalomethoxy, trihalocarbon, thioalkyl, SO2alkyl, COO-alkyl, KH2, OH, CN, SO2X5, NO2, NO, C═SR2 NSO2X5, C═OR2, where X5 is F, NH2, alkyl or H, and R2 is alkyl, NH2, NH-alkyl or O-alkyl, C1 to C6 alkyl or alkoxy; or wherein X1 has the formula —O—(CH2)n—O—, wherein n is an integer from 0 to 2, preferably 1 or 2, and one of the oxygens is bonded at the 5′-position and the other at the 4′-position of the aryl ring. The compounds are useful in cancer therapy and as radioimaging ligands.
摘要翻译：具有式（I）的右侧芳基部分具有2'，4'，5'-取代模式的Hsp90抑制剂。 X1表示在芳基的4'和5'位置上可以相同或不同的两个取代基，其中X 1选自卤素，烷基，烷氧基，卤代烷氧基，羟基烷基，吡咯基，任选取代的芳氧基，烷基氨基，二烷基氨基，氨基甲酰基，酰胺基，烷基酰氨基二酰氨基，酰基氨基，烷基磺酰氨基，三卤甲氧基，三卤代，硫代烷基，SO 2烷基，COO-烷基，KH 2，OH，CN，SO 2 X 5，NO 2，NO，C≡SR2 NSO 2 X 5，C = OR 2，其中X 5为 F，NH 2，烷基或H，并且R 2是烷基，NH 2，NH-烷基或O-烷基，C 1至C 6烷基或烷氧基; 或其中X 1具有式-O-（CH 2）n -O-，其中n为0至2的整数，优选1或2，并且其中一个氧键在5'-位上而另一个在芳基环的4'-位。该化合物可用于癌症治疗和放射成像配体。

4. 发明申请

US20200237934A1 HSP90-TARGETED INFLAMMATION AND INFECTION IMAGING AND THERAPY 审中-公开
公开(公告)号：US20200237934A1
公开(公告)日：2020-07-30
申请号：US16845372
申请日：2020-04-10
申请人： Memorial Sloan Kettering Cancer Center
发明人： Mark Dunphy , Gabriela Chiosis
IPC分类号： A61K51/04 , A61K49/00 , A61P35/00 , A61K49/18 , A61K31/52 , A61B6/00 , A61B6/03 , A61B5/00 , A61B5/08 , A61B5/0402 , A61B5/0275
摘要： The present invention provides new methods for inflammation and infection imaging and related medical applications thereof. In some embodiments, the present invention provides a method for the diagnosis of inflammation and/or infection. In some embodiments, the present invention provides a method for the treatment or prevention of inflammation and/or infection. In some embodiments, the present invention provides methods for monitoring the effect of inflammation and/or infection treatment, and/or methods for monitoring an inflammation and/or infection treatment regimen. In some embodiments, the present invention provides a method for selecting subjects for an inflammation and/or infection treatment. In some embodiments, the present invention provides a method for determining the dosage of a drug for the treatment of inflammation and/or infection.

5. 发明授权

US10647683B2 Hsp70 modulators and methods for making and using the same 有权
公开(公告)号：US10647683B2
公开(公告)日：2020-05-12
申请号：US16179155
申请日：2018-11-02
申请人： Memorial Sloan Kettering Cancer Center
发明人： Gabriela Chiosis , Yanlong Kang , Hardik J. Patel , Maulik Patel , Stefan Ochiana , Anna Rodina , Tony Taldone , Liza Shrestha
IPC分类号： C07D239/46 , C07D401/12 , C07D239/42 , C07D413/12 , A61K31/506 , A61K31/5377 , A61K45/06 , C07D403/04 , C07D405/12 , C07D407/12 , C07D417/12
摘要： The present invention, among other things, provides compounds and compositions thereof for use in the modulation of Hsp70. In some embodiments, the present invention provides a method for inhibiting Hsp70 activity. In some embodiments, the present invention provides a method of treating a subject suffering from or susceptible to a disease, disorder, or condition responsive to Hsp70 inhibition comprising administering to the subject a therapeutically effective amount of a provided compound. In some embodiments, the present invention provides a method for treating or preventing cancer in a subject suffering therefrom, comprising administering to a patient in need thereof a therapeutically effective amount of a provided compound.

6. 发明申请

US20200017502A1 METHODS AND REAGENTS FOR RADIOLABELING 审中-公开
公开(公告)号：US20200017502A1
公开(公告)日：2020-01-16
申请号：US16396496
申请日：2019-04-26
申请人： Memorial Sloan-Kettering Cancer Center
发明人： Stefan O. Ochiana , NagaVaraKishore Pillarsetty , Tony Taldone , Gabriela Chiosis
IPC分类号： C07D473/34 , C07F7/22 , C07B59/00
摘要： The present invention provides methods for radiolabeling compounds useful as Hsp90 inhibitors. The present invention also provides intermediates useful in such methods, and compositions of radiolabeled compounds. The present invention provides, among other things novel methods for the synthesis of radiolabeled compounds. In certain embodiments, the present invention provides compounds of formula I.

7. 发明授权

US10421758B2 Selective Grp94 inhibitors and uses thereof 有权
公开(公告)号：US10421758B2
公开(公告)日：2019-09-24
申请号：US14912082
申请日：2014-08-15
申请人： Memorial Sloan-Kettering Cancer Center
发明人： Gabriela Chiosis , Pengrong Yan , Pallav Patel , Hardik J. Patel , Tony Taldone , Chenghua Yang , Weilin Sun , Stefan O. Ochiana
IPC分类号： C40B30/02 , G01N33/50 , C07D473/34 , C07D519/00 , G16B35/00 , G16C20/60
摘要： The disclosure relates to novel selective Grp94 inhibitors, compositions comprising an effective amount of such compounds, and methods to treat or prevent a condition, such as cancer, comprising administering to an animal in need thereof an effective amount of such compounds.

8. 发明申请

US20190241526A1 HSP70 MODULATORS AND METHODS FOR MAKING AND USING THE SAME 审中-公开
公开(公告)号：US20190241526A1
公开(公告)日：2019-08-08
申请号：US16179155
申请日：2018-11-02
申请人： Memorial Sloan Kettering Cancer Center
发明人： Gabriela Chiosis , Yanlong Kang , Hardik J. Patel , Maulik Patel , Stefan Ochiana , Anna Rodina , Tony Taldone , Liza Shrestha
IPC分类号： C07D239/46 , C07D417/12 , C07D407/12 , A61K31/506 , A61K31/5377 , C07D401/12 , C07D403/04 , C07D405/12 , C07D413/12 , C07D239/42 , A61K45/06
CPC分类号： C07D239/46 , A61K31/506 , A61K31/5377 , A61K45/06 , C07D239/42 , C07D401/12 , C07D403/04 , C07D405/12 , C07D407/12 , C07D413/12 , C07D417/12
摘要： The present invention, among other things, provides compounds and compositions thereof for use in the modulation of Hsp70. In some embodiments, the present invention provides a method for inhibiting Hsp70 activity. In some embodiments, the present invention provides a method of treating a subject suffering from or susceptible to a disease, disorder, or condition responsive to Hsp70 inhibition comprising administering to the subject a therapeutically effective amount of a provided compound. In some embodiments, the present invention provides a method for treating or preventing cancer in a subject suffering therefrom, comprising administering to a patient in need thereof a therapeutically effective amount of a provided compound.

9. 发明申请

US20180251461A1 METHODS AND REAGENTS FOR RADIOLABELING 审中-公开
公开(公告)号：US20180251461A1
公开(公告)日：2018-09-06
申请号：US15971908
申请日：2018-05-04
申请人： Memorial Sloan-Kettering Cancer Center
发明人： Stefan O. Ochiana , NagaVaraKishore Pillarsetty , Tony Taldone , Gabriela Chiosis
IPC分类号： C07D473/34 , C07B59/00 , C07F7/22
CPC分类号： C07D473/34 , C07B59/002 , C07B2200/05 , C07F7/2208
摘要： The present invention provides methods for radiolabeling compounds useful as Hsp90 inhibitors. The present invention also provides intermediates useful in such methods, and compositions of radiolabeled compounds. The present invention provides, among other things novel methods for the synthesis of radiolabeled compounds. In certain embodiments, the present invention provides compounds of formula I.

10. 发明授权

US11065350B2 HSP90-targeted inflammation and infection imaging and therapy 有权
公开(公告)号：US11065350B2
公开(公告)日：2021-07-20
申请号：US16845372
申请日：2020-04-10
申请人： Memorial Sloan Kettering Cancer Center
发明人： Mark Dunphy , Gabriela Chiosis
IPC分类号： A61K51/04 , A61P35/00 , A61K49/00 , A61B5/00 , A61K31/52 , A61B5/318 , A61B5/0275 , A61B5/08 , A61B6/03 , A61B6/00 , A61K49/18
摘要： The present invention provides new methods for inflammation and infection imaging and related medical applications thereof. In some embodiments, the present invention provides a method for the diagnosis of inflammation and/or infection. In some embodiments, the present invention provides a method for the treatment or prevention of inflammation and/or infection. In some embodiments, the present invention provides methods for monitoring the effect of inflammation and/or infection treatment, and/or methods for monitoring an inflammation and/or infection treatment regimen. In some embodiments, the present invention provides a method for selecting subjects for an inflammation and/or infection treatment. In some embodiments, the present invention provides a method for determining the dosage of a drug for the treatment of inflammation and/or infection.

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