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公开(公告)号：US20210024504A1
公开(公告)日：2021-01-28
申请号：US16936022
申请日：2020-07-22
发明人： Rajan Kumar PAL , Biswajit SAMANTA , Jayraj Dilipbhai ARADHYE , Sandeep Pankajkumar PATHAK , Kaushik Dhanjibhai PRAJAPATI , Bhavesh Mohanbhai PANCHAL , Trinadha Rao CHITTURI
IPC分类号： C07D405/10 , A61P35/00
摘要： A selective estrogen receptor degrader (SERD), a compound 3-(3,5-difluorophenyl)-2-[4-[(E)-3-[3-(fluoromethyl)azetidin-1-yl]prop-1-enyl]phenyl]-4-methyl-2H-chromen-7-ol, and its S enantiomer, (2S)-3-(3,5-difluorophenyl)-2-[4-[(E)-3-[3-(fluoromethyl)azetidin-1-yl]prop-1-enyl]phenyl]-4-methyl-2H-chromen-7-ol, or pharmaceutically acceptable salts thereof. Also provided are processes for their preparation. Also provided for is the use of these compounds for the treatment of diseases which are related to modulation of estrogen receptors, such as ER-positive breast cancer.
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公开(公告)号：US20180354936A1
公开(公告)日：2018-12-13
申请号：US15770824
申请日：2016-10-26
发明人： Ranjan Kumar PAL , Amit Pravinbhai SEDANI , Kaushikkumar Dhanjibhai PRAJAPATI , Dijixa Pinakin RANA , Sandeep Pankajbhai PATHAK , Japan Nitinkumar DESAI , Jayraj Dilipbhai ARADHYE , Bhavesh Mohanbhai PANCHAL , Indraneel GHOSH , Trinadha Rao CHITTURI
IPC分类号： C07D405/10 , C07D311/60
CPC分类号： C07D405/10 , C07D215/12 , C07D311/60 , C07D335/06
摘要： The present invention provides novel heterocyclic compounds as anticancer agents, especially as estrogen receptor (ER) antagonists/degraders and process for their preparation.
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公开(公告)号：US20210261534A1
公开(公告)日：2021-08-26
申请号：US17308501
申请日：2021-05-05
发明人： Ranjan Kumar PAL , Biswajit SAMANTA , Jayraj Dilipbhai ARADHYE , Sandeep Pankajkumar PATHAK , Kaushik Dhanjibhai PRAJAPATI , Bhavesh Mohanbhai PANCHAL , Trinadha Rao CHITTURI
IPC分类号： C07D405/10 , A61P35/00
摘要： A selective estrogen receptor degrader (SERD), a compound 3-(3,5-difluorophenyl)-2-[4-[(E)-3-[3-(fluoromethyl)azetidin-1-yl]prop-1-enyl]phenyl]-4-methyl-2H-chromen-7-ol, and its S enantiomer, (2S)-3-(3,5-difluorophenyl)-2-[4-[(E)-3-[3-(fluoromethyl)azetidin-1-yl]prop-1-enyl]phenyl]-4-methyl-2H-chromen-7-ol, or pharmaceutically acceptable salts thereof. Also provided are processes for their preparation. Also provided for is the use of these compounds for the treatment of diseases which are related to modulation of estrogen receptors, such as ER-positive breast cancer.
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公开(公告)号：US20210053947A1
公开(公告)日：2021-02-25
申请号：US17082488
申请日：2020-10-28
发明人： Rajan Kumar PAL , Amit Pravinbhai SEDANI , Kaushikkumar Dhanjibhai PRAJAPATI , Dijixa Pinakin RANA , Sandeep Pankajbhai PATHAK , Japan Nitinkumar DESAI , Jayraj Dilipbhai ARADHYE , Bhavesh Mohanbhai PANCHAL , Indraneel GHOSH , Trinadha Rao CHITTURI
IPC分类号： C07D405/10 , C07D311/60 , C07D335/06 , C07D215/12
摘要： The present invention provides novel heterocyclic compounds as anticancer agents, especially as estrogen receptor (ER) antagonists/degraders and process for their preparation.
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公开(公告)号：US20220242874A1
公开(公告)日：2022-08-04
申请号：US17625960
申请日：2020-07-13
发明人： Jiten Ranchhodbhai PATEL , Gopalkumar Chimanlal PATEL , Omkar Prakash GORE , Prabal SENGUPTA , Trinadha Rao CHITTURI
IPC分类号： C07D491/22 , A61P35/00
摘要： A compound of Formula I or a pharmaceutically acceptable salt thereof (wherein X, Y, Z and n are defined herein). These compounds are useful in the treatment of diseases mediated by topoisomerase I enzyme such as cancers. Also provided are processes for the preparation of compounds of Formula I. The compounds are more water soluble, stable in buffer solution at various pH, and exhibit better anti-tumor activity and rapid release of SN-38 in tumor microenvironments.
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公开(公告)号：US20190275017A1
公开(公告)日：2019-09-12
申请号：US16304914
申请日：2017-06-02
发明人： Nitin Krishnaji DAMLE , Sanjay Nandlalji MANDHANE , Manoj Atmaramji UPADHYA , Sameer Vishwanath MEHETRE , Gajanan Uttamrao CHIDREWAR , Prabal SENGUPTA , Trinadha Rao CHITTURI
摘要： The invention relates to a method of treating or preventing Parkinson's disease in a subject comprising administering a compound of Formula I wherein, R1 is —NHC(O) C3-6 cycloalkyl and R2 is hydrogen; or R1 and R2 along with the carbon atoms to which they are attached form a six membered aromatic ring, wherein the ring is substituted with one or more groups selected from hydrogen, halogen and C1-6 alkyl; R3 and R4 are independently selected from group comprising hydrogen, halogen, C1-3 alkyl, OC1-3 alkyl, NO2, SC1-3, alkyl, C1-3, haloalkyl, OC1-3 haloalkyl, and SC1-3 haloalkyl; or a pharmaceutically acceptable salt thereof.
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