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1. 发明申请

WO2022084930A2 CANCER THERAPY USING A COMBINATION OF CDK7 INHIBITOR WITH AN ANTI-MICROTUBULE AGENT 审中-公开
公开(公告)号：WO2022084930A2
公开(公告)日：2022-04-28
申请号：PCT/IB2021/059751
申请日：2021-10-22
申请人： AURIGENE DISCOVERY TECHNOLOGIES LIMITED
发明人： KUMAR, Akhil , NARAYANAN, Kishore , PODDUTOORI, Ramulu
IPC分类号： A61K31/00
摘要： The present invention provides a combination of a substituted heterocyclyl derivative of formula (I) or a pharmaceutically acceptable salt thereof which is a CDK7 inhibitor along with an anti-microtubule agent or prodrug thereof, and a method of treating or preventing cancer in a subject, comprising administering to the subject a compound of formula (I) conjointly with the anti-microtubule agent.

2. 发明申请

WO2019207538A1 PYRIDAZINE DERIVATIVES AS SMARCA2/4 DEGRADERS 审中-公开
公开(公告)号：WO2019207538A1
公开(公告)日：2019-10-31
申请号：PCT/IB2019/053443
申请日：2019-04-26
申请人： AURIGENE DISCOVERY TECHNOLOGIES LIMITED
发明人： SASMAL, Sanjita , SAMAJDAR, Susanta , MUKHERJEE, Subhendu , ABBINENI, Chandrasekhar
IPC分类号： C07D413/00 , C07D413/12 , A61K31/50
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 comprising at least one of the pyridazine derivatives of formula (I) or a pharmaceutically acceptable salt, or a stereoisomer thereof.

3. 发明申请

WO2018051254A1 CYCLIC SUBSTITUTED-1,2,4-OXADIAZOLE COMPOUNDS AS IMMUNOMODULATORS 审中-公开
标题翻译：作为免疫调节剂的环状取代-1,2,4-恶二唑化合物
公开(公告)号：WO2018051254A1
公开(公告)日：2018-03-22
申请号：PCT/IB2017/055546
申请日：2017-09-14
申请人： AURIGENE DISCOVERY TECHNOLOGIES LIMITED
发明人： SASIKUMAR, Pottayil Govindan Nair , PRASAD, Appukkuttan , NAREMADDEPALLI, Seetharamaiah Setty Sudarshan , RAMACHANDRA, Muralidhara
IPC分类号： C07D291/00 , C07D271/06 , C07D285/08 , A61K31/4245 , A61K31/433
CPC分类号： C07D271/06 , C07D271/07 , C07D413/04 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/14
摘要： The present invention relates to cyclic substituted-1,2,4-oxadiazole compounds of formula (I) and their use to inhibit the programmed cell death 1 (PD1) signalling pathway and/or for treatment of disorders by inhibiting an immunosuppressive signal induced by PD-1, PD-L1 or PD-L2.
摘要翻译：本发明涉及式（I）的环状取代的-1,2,4-恶二唑化合物及其用于抑制程序性细胞死亡1（PD1）信号传导途径和/或用于治疗通过抑制由PD-1，PD-L1或PD-L2诱导的免疫抑制信号引起的疾病。

4. 发明申请

WO2016185342A1 SUBSTITUTED TETRAHYDROQUINOLINONE COMPOUNDS AS ROR GAMMA MODULATORS 审中-公开
标题翻译：取代的四氢喹啉酮化合物作为ROR伽玛调制剂
公开(公告)号：WO2016185342A1
公开(公告)日：2016-11-24
申请号：PCT/IB2016/052773
申请日：2016-05-13
申请人： AURIGENE DISCOVERY TECHNOLOGIES LIMITED
发明人： KOTRABASAIAH UJJINAMATADA, Ravi , PANDIT, Chetan
IPC分类号： C07D215/36
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.
摘要翻译：本发明提供取代的四氢喹啉酮和相关的式（I）化合物，其可用作视黄酸受体相关孤儿受体（ROR）的调节剂，更特别地作为RORγ调节剂。这些化合物可用于治疗和预防疾病和/或病症，特别是它们在由RORγ受体介导的疾病和/或障碍中的用途。本发明还提供包含至少一种取代的四氢喹啉酮或式（I）的相关化合物及其可药用载体，稀释剂或赋形剂的化合物和药物制剂的制备。

5. 发明申请

WO2016142855A2 PYRAZOLO[1,5-A][1,3,5]TRIAZINE AND PYRAZOLO[1,5-A]PYRIMIDINE DERIVATIVES AS CDK INHIBITORS 审中-公开
标题翻译：吡咯并[1,5-A] [1,3,5]三嗪和吡唑并[1,5-A]吡嗪衍生物作为CDK抑制剂
公开(公告)号：WO2016142855A2
公开(公告)日：2016-09-15
申请号：PCT/IB2016/051302
申请日：2016-03-08
申请人： AURIGENE DISCOVERY TECHNOLOGIES LIMITED
发明人： SAMAJDAR, Susanta , PODDUTOORI, Ramulu , MUKHERJEE, Subhendu , GOSWAMI, Rajeev
IPC分类号： A61K31/437
CPC分类号： C07D487/04 , A61K31/53 , A61K45/06
摘要： The present invention provides substituted pyrazolo[1,5-a][1,3,5]triazine and pyrazolo[1,5-a]pyrimidine derivatives of formula (I), which are therapeutically useful, particularly as selective transcriptional CDK inhibitors including CDK7, CDK9, CDK12, CDK13 and CDK18, more particularly transcriptional CDK7 inhibitors wherein X, ring A, ring B, L1, L2, R1,R2, R3, R4, R6, m, n and p have the meanings given in the specification and pharmaceutically acceptable salts thereof that are useful in the treatment and prevention of diseases or disorder associated with selective transcriptional CDKs in a mammal. The present invention also provides preparation of the compounds and pharmaceutical formulations comprising at least one of the substituted pyrazolo[1,5-a][1,3,5]triazine and pyrazolo[1,5-a]pyrimidine derivatives of formula (I) or a pharmaceutically acceptable salt thereof or a stereoisomer thereof.
摘要翻译：本发明提供了治疗上有用的取代的吡唑并[1,5-a] [1,3,5]三嗪和吡唑并[1,5-a]嘧啶衍生物，特别是选择性转录CDK抑制剂，包括 CDK7，CDK9，CDK12，CDK13和CDK18，更特别是转录CDK7抑制剂，其中X，环A，环B，L1，L2，R1，R2，R3，R4，R6，m，n和p具有本说明书和其药学上可接受的盐，其可用于治疗和预防与哺乳动物中选择性转录CDK相关的疾病或病症。本发明还提供包含式（I）的取代的吡唑并[1,5-a] [1,3,5]三嗪和吡唑并[1,5-a]嘧啶衍生物中的至少一种的化合物和药物制剂的制备）或其药学上可接受的盐或其立体异构体。

6. 发明申请

WO2015193846A1 SUBSTITUTED INDAZOLE COMPOUNDS AS IRAK4 INHIBITORS 审中-公开
标题翻译：取代的吲哚酮化合物作为IRAK4抑制剂
公开(公告)号：WO2015193846A1
公开(公告)日：2015-12-23
申请号：PCT/IB2015/054620
申请日：2015-06-19
申请人： AURIGENE DISCOVERY TECHNOLOGIES LIMITED
发明人： GUMMADI, Venkateshwar Rao , SAMAJDAR, Susanta
IPC分类号： A61K31/416 , C07D231/56 , C07D405/14 , C07D401/14 , A61P35/00
CPC分类号： C07D487/04 , C07D401/14 , C07D405/14 , C07D413/14 , C07D471/04
摘要： The present invention provides substituted indazole compound of formula (I) and pharmaceutically acceptable salts thereof, and their use to inhibit IRAK4 and/or for the treatment of diseases or disorders induced by IRAK4.
摘要翻译：本发明提供式（I）的取代的吲唑化合物及其药学上可接受的盐及其用于抑制IRAK4和/或用于治疗由IRAK4诱导的疾病或病症的用途。

7. 发明申请

WO2015071780A1 ALKYLIDINE SUBSTITUTED HETEROCYCLYL DERIVATIVES AS ANTI-BACTERIAL AGENTS 审中-公开
标题翻译：作为抗菌剂的烷基取代的杂环衍生物
公开(公告)号：WO2015071780A1
公开(公告)日：2015-05-21
申请号：PCT/IB2014/061104
申请日：2014-04-30
申请人： AURIGENE DISCOVERY TECHNOLOGIES LIMITED , UM PHARMAUJI SDN. BHD
发明人： MOHAMED, Takhi , HOSAHALLI, Subramanya , PANIGRAHI, Sunil Kumar
IPC分类号： A61K31/00
CPC分类号： C07D471/04
摘要： The present invention relates to alkylidine substituted heterocyclyl derivatives of formula (1) which may be therapeutically useful as as anti-bacterial agents, more particulalrly FabI inhibitors; I in which P, Q, Ri, R2, R3 and "n" have the same meanings given in the specification, and pharmaceutically acceptable salts or pharmaceutically acceptable stereoisomers thereof that are useful in the treatment and prevention in diseases or disorder, in particular their use in diseases or disorder where there is an advantage in inhibiting Enoyl-ACP reductase enzyme (FABI) activity. The present invention also provides methods for synthesizing and administering the FabI inhibitory compounds. The present invention also provides pharmaceutical formulations comprising at least one of the FabI inhibitory compounds together with a pharmaceutically acceptable carrier, diluent or excipient therefor.
摘要翻译：本发明涉及式（1）的烷基胺取代的杂环基衍生物，其可以作为抗细菌剂，更特别是FabI抑制剂; 其中P，Q，R 1，R 2，R 3和“n”具有与说明书中给出的相同的含义及其药学上可接受的盐或药学上可接受的立体异构体，其可用于治疗和预防疾病或病症，用于抑制Enoyl-ACP还原酶（FABI）活性有优势的疾病或病症。本发明还提供了合成和施用FabI抑制化合物的方法。本发明还提供了包含至少一种FabI抑制化合物及其药学上可接受的载体，稀释剂或赋形剂的药物制剂。

8. 发明申请

WO2014128655A1 SUBSTITUTED IMIDAZO[4,5-C]QUINOLINE DERIVATIVES AS BROMODOMAIN INHIBITORS 审中-公开
标题翻译：取代的咪唑并[4,5-C]喹啉衍生物作为BROMODOMAIN抑制剂
公开(公告)号：WO2014128655A1
公开(公告)日：2014-08-28
申请号：PCT/IB2014/059152
申请日：2014-02-21
申请人： AURIGENE DISCOVERY TECHNOLOGIES LIMITED
发明人： SASMAL, Sanjita , HOSAHALLI, Subramanya
IPC分类号： C07D519/00 , A61K31/4188 , A61K31/422 , A61P29/00 , A61P35/00 , A61P37/00
CPC分类号： C07D471/04
摘要： The present invention provides novel substituted imidazo[4,5-c]quinoline derivatives of formula (1), which may be therapeutically useful, more particularly as Bromodomain inhibitors; (1) in which Cy i , Cy 2 , R 1 , R 2 , R 3 , R 4 and R 5 have the same meanings given in the specification, and pharmaceutically acceptable salts thereof that are useful in the treatment and prevention of diseases or disorder, in particular their use in diseases or disorder associated as bromodomain inhibitors. The present invention also provides preparation of the compounds and pharmaceutical formulations comprising at least one of the substituted imidazo[4,5-C]quinoline compounds of formula (1) together with a pharmaceutically acceptable carrier, diluent or excipient therefor.
摘要翻译：本发明提供式（1）的新的取代的咪唑并[4,5-c]喹啉衍生物，其可以是治疗上有用的，更特别是作为溴代葡萄糖苷抑制剂; （1）其中Cy1，Cy2，R1，R2，R3，R4和R5与说明书中给出的相同含义及其药学上可接受的盐可用于治疗和预防疾病或病症，特别是其用于与溴结构域抑制剂相关的疾病或病症。本发明还提供包含至少一种式（1）的取代的咪唑并[4,5-C]喹啉化合物及其药学上可接受的载体，稀释剂或赋形剂的化合物和药物制剂的制备。

9. 发明申请

WO2013144704A1 IMMUNOMODULATING CYCLIC COMPOUNDS FROM THE BC LOOP OF HUMAN PD1 审中-公开
标题翻译：人PD1的BC循环免疫调节循环化合物
公开(公告)号：WO2013144704A1
公开(公告)日：2013-10-03
申请号：PCT/IB2013/000553
申请日：2013-03-28
申请人： AURIGENE DISCOVERY TECHNOLOGIES LIMITED
发明人： SASIKUMAR, Pottayil Govindan Nair , RAMACHANDRA, Muralidhara
IPC分类号： C07K14/705 , C07K14/47 , A61K38/00
CPC分类号： C07K7/64 , A61K31/395 , A61K38/00 , A61K38/12 , A61K45/06 , C07K14/4747 , C07K14/70503 , A61K2300/00
摘要： The present invention relates to novel cyclic compounds as therapeutic agents capable of inhibiting the programmed cell death 1 (PD1) signalling pathway. The invention also relates to derivative's 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.
摘要翻译：本发明涉及作为能够抑制程序性细胞死亡1（PD1）信号传导途径的治疗剂的新型环状化合物。本发明还涉及治疗剂的衍生物。本发明还包括所述治疗剂和衍生物用于通过免疫激活治疗疾病的用途，包括抑制由于PD-1，PD-L1或PD-L2引起的免疫抑制信号和使用它们的疗法。

10. 发明申请

WO2013080222A1 SUBSTITUTED PYRIDINE DERIVATIVES AS FABI INHIBITORS 审中-公开
标题翻译：取代的吡啶衍生物作为FABI抑制剂
公开(公告)号：WO2013080222A1
公开(公告)日：2013-06-06
申请号：PCT/IN2012/000776
申请日：2012-11-29
申请人： AURIGENE DISCOVERY TECHNOLOGIES LIMITED
发明人： TAKHI, Mohamed , HOSAHALLI, Subramanya , PANIGRAHI, Sunil Kumar , MAHADARI, Muni Kumar , KOTTAM, Chandrashekar Reddy , ABD RAHMAN, Noorsaadah , YUSOF, Rohana
IPC分类号： C07D471/04 , C07D471/14 , A61K31/4375 , A61K31/438 , A61K31/5513 , A61K31/519 , A61P31/04
CPC分类号： C07D213/75 , C07D401/14 , C07D471/04 , C07D471/14 , C07D471/20 , C07F5/025
摘要： The present invention provides substituted pyridine derivatives of formula (I), which may be therapeutically useful as as anti-bacterial agents, more particulalrly FabI inhibitors. Formula(I) in which R1 to R5 and L have the meanings given in the specification, and pharmaceutically acceptable salts thereof that are useful in the treatment and prevention in diseases or disorder, in particular their use in diseases or disorder where there is an advantage anti-bacterial agents, more particularly FabI inhibitors. The present invention also provides methods for synthesizing and administering the FabI inhibitor compounds. The present invention also provides pharmaceutical formulations comprising at least one of the FabI inhibitor compounds together with a pharmaceutically acceptable carrier, diluent or excipient therefor.
摘要翻译：本发明提供式（I）的取代的吡啶衍生物，其可以作为抗细菌剂，更特别是FabI抑制剂是治疗上有用的。其中R1至R5和L具有本说明书中给出的含义的式（I）及其可用于治疗和预防疾病或病症的药学上可接受的盐，特别是其在有优势的疾病或病症中的用途抗菌剂，更特别是FabI抑制剂。本发明还提供了合成和施用FabI抑制剂化合物的方法。本发明还提供了包含至少一种FabI抑制剂化合物与药学上可接受的载体，稀释剂或赋形剂的药物制剂。

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