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公开(公告)号：US20230110077A1
公开(公告)日：2023-04-13
申请号：US17962976
申请日：2022-10-10
发明人： Pottayil Govindan N. Sasikumar , Muralidhara Ramachandra , Seetharamaiah Setty Sudarshan Naremaddepalli
IPC分类号： C07D271/06 , C07D413/04 , C07D413/06 , C07D413/12 , C07D271/10 , C07K5/087 , A61P35/00 , A61K31/4245 , A61K38/05 , A61K45/06 , C07K5/065
摘要： The present invention relates to 1,2,4-oxadiazole and thiadiazole compounds of formula (I) and their use to inhibit the programmed cell death 1 (PD1) signaling pathway and/or for treatment of disorders by inhibiting an immunosuppressive signal induced by PD-1, PD-L1 or PD-L2.
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公开(公告)号：US20230027075A1
公开(公告)日：2023-01-26
申请号：US17779973
申请日：2020-11-26
发明人： Susanta SAMAJDAR , Dinesh CHIKKANNA , Sunil Kumar PANIGRAHI , Chandregowda VENKATESHAPPA , Garima PRIYADARSHANI
IPC分类号： C07D487/04
摘要： The present invention relates to bispecific compound of formula (I) as dual inhibitors of CD73 and adenosine receptors. The present invention also relates to pharmaceutical compositions comprising said compounds or a pharmaceutically acceptable salt or a stereoisomer or a prodrug thereof and use of such compounds in the treatment of diseases mediated by CD73 and/or adenosine receptors, particularly A2aR or A2bR.
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公开(公告)号：US11365205B2
公开(公告)日：2022-06-21
申请号：US16982996
申请日：2019-03-20
发明人： Dinesh Chikkanna , Sunil Kumar Panigrahi , Srinivasa Raju Sammeta , Wohlfahrt Gerd , Myllymaki Mikko
IPC分类号： C07D401/14 , A61K31/4725 , C07D498/08 , A61P35/00 , C07D401/06 , C07D405/14 , C07D413/14 , C07D471/04
摘要： The present invention relates to the derivatives of compound of formula (I) and pharmaceutically acceptable salts thereof. The present invention further provides the methods of preparation of compound of formula (I) and use thereof as PRMT5 inhibitors. The compounds are useful as medicaments in the treatment of conditions where PRMT5 inhibition is desired, such as cancer, metabolic disorders, inflammation, autoimmune disease and hemoglobinopathies.
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公开(公告)号：US20220125780A1
公开(公告)日：2022-04-28
申请号：US17570693
申请日：2022-01-07
IPC分类号： A61K31/4709 , C07D403/04 , C07D401/14 , C07D401/04 , C07D409/04 , C07D239/26 , C07D487/04 , C07D405/04 , A61K31/4985 , A61K31/501 , A61K31/506
摘要： The present invention provides substituted tetrahydroquinolinone and related compounds of formula (I), which are therapeutically useful as modulators of Retinoic acid receptor-related orphan receptors (RORs), more particularly as RORγ modulators. These compounds are useful in the treatment and prevention of diseases and/or disorder, in particular their use in diseases and/or disorder mediated by RORγ receptor. The present invention also provides preparation of the compounds and pharmaceutical formulations comprising at least one of the substituted tetrahydroquinolinone or related compounds of formula (I), together with a pharmaceutically acceptable carrier, diluent or excipient therefor.
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公开(公告)号：US20210253564A1
公开(公告)日：2021-08-19
申请号：US17050792
申请日：2019-04-26
IPC分类号： C07D413/14 , C07D401/14 , C07D487/08
摘要： The present invention provides pyridazine derivatives of formula (I), which are therapeutically useful as SMARCA2/4 degraders. These compounds are useful in the treatment and/or prevention of diseases or disorders dependent upon SMARCA2/4 in a mammal. The present invention also provides preparation of the compounds and pharmaceutical compositions of at least one of the pyridazine derivatives of formula (I) or a pharmaceutically acceptable salt, or a stereoisomer thereof.
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公开(公告)号：US20210002299A1
公开(公告)日：2021-01-07
申请号：US16982996
申请日：2019-03-20
发明人： Dinesh CHIKKANNA , Sunil Kumar PANIGRAHI , Srinivasa Raju SAMMETA , Wohlfahrt GERD , Myllymaki MIKKO
IPC分类号： C07D498/08 , C07D401/14 , C07D401/06 , C07D413/14 , C07D405/14 , C07D471/04 , A61P35/00
摘要： The present invention relates to the derivatives of compound of formula (I) and pharmaceutically acceptable salts thereof. The present invention further provides the methods of preparation of compound of formula (I) and use thereof as PRMT5 inhibitors. The compounds are useful as medicaments in the treatment of conditions where PRMT5 inhibition is desired, such as cancer, metabolic disorders, inflammation, autoimmune disease and hemoglobinopathies.
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公开(公告)号：US20180200247A1
公开(公告)日：2018-07-19
申请号：US15574243
申请日：2016-05-13
IPC分类号： A61K31/4709 , A61K31/4985 , A61K31/506 , A61K31/501
CPC分类号： A61K31/4709 , A61K31/4985 , A61K31/501 , A61K31/506 , C07D239/26 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/04 , C07D409/04 , C07D487/04
摘要： The present invention provides substituted tetrahydroquinolinone and related compounds of formula (I), which are therapeutically useful as modulators of Retinoic acid receptor-related orphan receptors (RORs), more particularly as RORγ modulators. These compounds are useful in the treatment and prevention of diseases and/or disorder, in particular their use in diseases and/or disorder mediated by RORγ receptor. The present invention also provides preparation of the compounds and pharmaceutical formulations comprising at least one of the substituted tetrahydroquinolinone or related compounds of formula (I), together with a pharmaceutically acceptable carrier, diluent or excipient therefor.
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公开(公告)号：US20180086726A1
公开(公告)日：2018-03-29
申请号：US15722194
申请日：2017-10-02
申请人： Pottayil Govindan Nair Sasikumar , Muralidhara Ramachandra , Seetharamaiah Setty Sudarshan Naremaddepalli
发明人： Pottayil Govindan Nair Sasikumar , Muralidhara Ramachandra , Seetharamaiah Setty Sudarshan Naremaddepalli
IPC分类号： C07D285/12 , A61K31/433 , A61K45/06 , A61K31/4245 , C07D271/10
CPC分类号： C07D285/12 , A61K31/4245 , A61K31/433 , A61K45/06 , A61P31/00 , A61P35/00 , C07D271/10
摘要： The present invention relates to synthetic methods for 1,3,4-oxadiazole and 1,3,4-thiadiazole compounds. The general synthetic scheme is: R1 substituents are —CH2OH, —CH(CH3)OH, —CH2Ph, —CH3, or —CH2C(O)NH2 optionally substituted with alkyl or aralkyl. R3 substituents are —CH2OH, —CH3, —CH2CH2C(O)OH, —CH2CH2C(O)NH2, —CH2C(O)NH2, or —CH2C(O)OH, wherein the carboxylic acids and amides are optionally substituted with alkyl or aralkyl.
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公开(公告)号：US09776978B2
公开(公告)日：2017-10-03
申请号：US15296292
申请日：2016-10-18
申请人： Pottayil Govindan Nair Sasikumar , Muralidhara Ramachandra , Seetharamaiah Setty Sudarshan Naremaddepalli
发明人： Pottayil Govindan Nair Sasikumar , Muralidhara Ramachandra , Seetharamaiah Setty Sudarshan Naremaddepalli
IPC分类号： C07D285/12 , C07D271/10 , A61K31/433 , A61K45/06 , A61K31/4245
CPC分类号： C07D285/12 , A61K31/4245 , A61K31/433 , A61K45/06 , A61P31/00 , A61P35/00 , C07D271/10
摘要： The present invention relates to 1,3,4-oxadiazole and 1,3,4-thiadiazole compounds as therapeutic agents capable of inhibiting the programmed cell death 1 (PD1) signalling pathway. The invention also refers to derivatives of the therapeutic agents. The invention also encompasses the use of the said therapeutic agents and derivatives for treatment of disorders via immunopotentiation comprising inhibition of immunosuppressive signal induced due to PD-1, PD-L1, or PD-L2 and therapies using them.
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公开(公告)号：US09732095B2
公开(公告)日：2017-08-15
申请号：US15111000
申请日：2015-01-12
IPC分类号： C07D513/04 , C07D519/00 , C07D498/04
CPC分类号： C07D513/04 , C07D498/04 , C07D519/00
摘要： The present invention provides bicyclic heterocyclyl kinase enzyme inhibitor compounds of formula (I), which are therapeutically useful as kinase inhibitors, particularly IRAK4 inhibitors, wherein A, Y, Z, X1, X2, R1, R3, ‘m’, ‘n’ and ‘p’ have the meanings given in the specification and pharmaceutically acceptable salt or stereoisomer thereof that are useful in the treatment and prevention of diseases or disorder, in particular their use in diseases or disorder mediated by kinase enzyme, particularly IRAK4 enzyme. The present invention also provides pharmaceutical composition comprising at least one of the compounds of compound of formula (I) together with a pharmaceutically acceptable carrier, diluent or excipient therefor.
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