专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

WO2021005043A1 MACROCYCLIC SPIROCYCLE DERIVATIVES AS MCL-1 INHIBITORS 审中-公开
公开(公告)号：WO2021005043A1
公开(公告)日：2021-01-14
申请号：PCT/EP2020/069097
申请日：2020-07-07
申请人： JANSSEN PHARMACEUTICA NV
发明人： ROMBOUTS, Frederik, Jan, Rita , DIELS, Gaston, Stanislas, Marcella , JERHAOUI, Soufyan , SURKYN, Michel , VAN ROOSBROECK, Yves, Emiel, Maria
IPC分类号： C07D513/22 , A61P35/00 , A61K31/553 , C07D513/20
摘要： The present invention relates to pharmaceutical agents of formula (I) useful for therapy and/or prophylaxis in a subject, pharmaceutical composition comprising such compounds, and their use as MCL-1 inhibitors, useful for treating diseases such as cancer.

2. 发明申请

WO2020254471A1 MACROCYCLIC INHIBITORS OF MCL-1 审中-公开
公开(公告)号：WO2020254471A1
公开(公告)日：2020-12-24
申请号：PCT/EP2020/066890
申请日：2020-06-18
申请人： JANSSEN PHARMACEUTICA NV
发明人： ROMBOUTS, Frederik, Jan, Rita , PESCHIULLI, Aldo
IPC分类号： C07D515/22 , A61P35/00 , A61K31/395
摘要： The present invention relates to pharmaceutical agents useful for therapy and/or prophylaxis in a subject, pharmaceutical composition comprising such compounds, and their use as MCL-1 inhibitors, useful for treating diseases such as cancer.

3. 发明申请

WO2021255257A1 N-LINKED MACROCYCLIC 7-(PYRAZOL-5-YL)-INDOLE DERIVATIVES AS INHIBITORS OF MCL-1 审中-公开
公开(公告)号：WO2021255257A1
公开(公告)日：2021-12-23
申请号：PCT/EP2021/066653
申请日：2021-06-18
申请人： JANSSEN PHARMACEUTICA NV
发明人： ROMBOUTS, Frederik, Jan, Rita , DE BOECK, Benoît, Christian, Albert, Ghislain , PESCHIULLI, Aldo , VELTER, Adriana, Ingrid
IPC分类号： C07D498/22 , C07D515/22 , A61P35/00 , A61K31/4162
摘要： The present invention relates to pharmaceutical agents useful for therapy and/or prophylaxis in a subject, pharmaceutical composition comprising such compounds, and their use as MCL-1 inhibitors, useful for treating diseases such as cancer.

4. 发明申请

WO2021099579A1 MACROCYCLIC INDOLE DERIVATIVES AS MCL-1 INHIBITORS 审中-公开
公开(公告)号：WO2021099579A1
公开(公告)日：2021-05-27
申请号：PCT/EP2020/082900
申请日：2020-11-20
申请人： JANSSEN PHARMACEUTICA NV
发明人： ROMBOUTS, Frederik, Jan, Rita , DE BOECK, Benoît, Christian, Albert, Ghislain
IPC分类号： C07D515/22 , A61P35/00 , A61K31/395
摘要： The present invention relates to pharmaceutical agents useful for therapy and/or prophylaxis in a subject, pharmaceutical composition comprising such compounds, and their use as MCL-1 inhibitors, useful for treating diseases such as cancer.

5. 发明申请

WO2018083247A1 4,4A,5,7-TETRAHYDRO-3H-FURO[3,4-B]PYRIDINYL COMPOUNDS 审中-公开
标题翻译： 4,4A，5,7-四氢-3H-呋喃并[3,4-B]吡啶基化合物
公开(公告)号：WO2018083247A1
公开(公告)日：2018-05-11
申请号：PCT/EP2017/078200
申请日：2017-11-03
申请人： JANSSEN PHARMACEUTICA NV
发明人： VAN BRANDT, Sven, Franciscus, Anna , GIJSEN, Henricus, Jacobus, Maria , ROMBOUTS, Frederik, Jan, Rita
IPC分类号： C07D491/048 , A61K31/4355 , A61P25/28
摘要： The present invention relates to 4,4a,5,7-tetrahydro-3H-furo[3,4-b]pyridinyl compound inhibitors of beta-site APP-cleaving enzyme having the structure shown in Formula (I) wherein the radicals are as defined in the specification. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which beta-site APP- cleaving enzyme is involved, such as Alzheimer's disease (AD), mild cognitive impairment, preclinical Alzheimer's disease, senility, dementia, dementia with Lewy bodies, Down's syndrome, dementia associated with stroke, dementia associated with Parkinson's disease, and dementia associated with beta-amyloid.
摘要翻译：本发明涉及具有式（I）所示结构的β位APP剪切酶的4,4a，5,7-四氢-3H-呋喃并[3,4-b]吡啶基化合物抑制剂。（I）其中基团如说明书中所定义。本发明还涉及包含此类化合物的药物组合物，涉及用于制备此类化合物和组合物的方法，并且涉及此类化合物和组合物用于预防和治疗其中涉及β位APP裂解酶的疾病的用途，例如阿尔茨海默病（AD），轻度认知障碍，临床前阿尔茨海默氏病，衰老，痴呆，路易体痴呆，唐氏综合症，与中风相关的痴呆，与帕金森氏病有关的痴呆和与β-淀粉样蛋白相关的痴呆。

6. 发明申请

WO2013000924A1 1-ARYL-4-METHYL-[1,2,4]TRIAZOLO[4,3-a]QUINOXALINE DERIVATIVES 审中-公开
标题翻译： 1-芳基-4-甲基 - [1,2,4]三唑并[4,3-a]喹啉衍生物
公开(公告)号：WO2013000924A1
公开(公告)日：2013-01-03
申请号：PCT/EP2012/062381
申请日：2012-06-26
申请人： JANSSEN PHARMACEUTICA NV , ANDRÉS-GIL, José, Ignacio , ROMBOUTS, Frederik, Jan, Rita , TRABANCO-SUÁREZ, Andrés, Avelino , VANHOOF, Greta, Constantia, Peter , DE ANGELIS, Meri , BUIJNSTERS, Peter, Jacobus, Johannes, Antonius , GUILLEMONT, Jerôme, Emile, Georges , BORMANS, Guy, Maurits R. , CELEN, Sofie, Jeanne, Leopoldine , VLIEGEN, Maarten
发明人： ANDRÉS-GIL, José, Ignacio , ROMBOUTS, Frederik, Jan, Rita , TRABANCO-SUÁREZ, Andrés, Avelino , VANHOOF, Greta, Constantia, Peter , DE ANGELIS, Meri , BUIJNSTERS, Peter, Jacobus, Johannes, Antonius , GUILLEMONT, Jerôme, Emile, Georges , BORMANS, Guy, Maurits R. , CELEN, Sofie, Jeanne, Leopoldine , VLIEGEN, Maarten
IPC分类号： C07D487/04 , A61K31/4985 , A61P25/00
CPC分类号： C07D487/04 , A61K31/4985 , A61K45/06 , A61K51/0463 , G01N33/60
摘要： The present invention relates to novel l-aryl-4-methyl-[l,2,4]triazolo[4,3-a]- quinoxaline derivatives as inhibitors of phosphodiesterase 2 (PDE2) and to a lesser extent of phosphodiesterase 10 (PDE10) or as inhibitors of both, phosphodiesterases 2 and 10. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which PDE2 is involved, or disorders in which both PDE2 and PDE10 are involved, such as neurological and psychiatric disorders, and endocrinological or metabolic diseases. The present invention also relates to radiolabeled compounds which may be useful for imaging and quantifying the PDE2 enzyme in tissues, using positron- emission tomography (PET). The invention is also directed to compositions comprising such compounds, to processes for preparing such compounds and compositions, to the use of such compounds and compositions for imaging a tissue, cells or a host, in vitro or in vivo and to precursors of said compounds.
摘要翻译：本发明涉及新的1-芳基-4-甲基 - [1,2,4]三唑并[4,3-a] - 喹喔啉衍生物作为磷酸二酯酶2（PDE2）的抑制剂，而较少程度的磷酸二酯酶10（PDE10 ）或作为磷酸二酯酶2和10两者的抑制剂。本发明还涉及包含这些化合物的药物组合物，制备此类化合物和组合物的方法，以及用于预防和治疗疾病的化合物和组合物其中涉及PDE2，或PDE2和PDE10都涉及的疾病，如神经和精神疾病，以及内分泌或代谢疾病。本发明还涉及放射性标记的化合物，其可用于使用正电子发射断层摄影（PET）在组织中成像和定量PDE2酶。本发明还涉及包含这些化合物的组合物，用于制备此类化合物和组合物的方法，以使用这些化合物和组合物用于在体外或体内成像组织，细胞或宿主以及所述化合物的前体。

7. 发明申请

WO2022229102A1 MACROCYCLIC 2-ALLYLTETRAHYDROFURANS AS INHIBITORS OF MCL-1 审中-公开
公开(公告)号：WO2022229102A1
公开(公告)日：2022-11-03
申请号：PCT/EP2022/060898
申请日：2022-04-25
申请人： JANSSEN PHARMACEUTICA NV
发明人： ROMBOUTS, Frederik, Jan, Rita , HSIAO, Meng-Yang , JERHAOUI, Soufyan , ROMANOV MICHAILIDIS, Fedor , SURKYN, Michel , URNER, Lorenz, Michael , DIELS, Gaston, Stanislas, M
IPC分类号： C07D513/20 , C07D513/22 , C07D519/00 , A61P35/00 , A61K31/553
摘要： The present invention relates to pharmaceutical agents useful for therapy and/or prophylaxis in a subject, pharmaceutical composition comprising such compounds, and their use as MCL-1 inhibitors, useful for treating diseases such as cancer.

8. 发明申请

WO2021239862A1 MACROCYCLIC 7-PYRAZOL-5-YL-INDOLE DERIVATIVES AS INHIBITORS OF MCL-1 审中-公开
公开(公告)号：WO2021239862A1
公开(公告)日：2021-12-02
申请号：PCT/EP2021/064162
申请日：2021-05-27
申请人： JANSSEN PHARMACEUTICA NV
发明人： ROMBOUTS, Frederik, Jan, Rita , PESCHIULLI, Aldo , DEMIN, Samuël, Dominique , VELTER, Adriana, Ingrid , JOUFFROY, Matthieu, Dominique
IPC分类号： C07D515/22 , A61P35/00 , A61K31/4162
摘要： The present invention relates to pharmaceutical agents useful for therapy and/or prophylaxis in a subject, pharmaceutical composition comprising such compounds, and their use as MCL-1 inhibitors, useful for treating diseases such as cancer.

9. 发明申请

WO2021165370A1 MACROCYCLIC INDOLE DERIVATIVES AS INHIBITORS OF MCL-1 审中-公开
公开(公告)号：WO2021165370A1
公开(公告)日：2021-08-26
申请号：PCT/EP2021/053973
申请日：2021-02-18
申请人： JANSSEN PHARMACEUTICA NV
发明人： ROMBOUTS, Frederik, Jan, Rita , REUILLON, Tristan , PESCHIULLI, Aldo , VELTER, Adriana, Ingrid , VOS, Ann, Marleen
IPC分类号： C07D515/22 , A61K31/395 , A61P35/00
摘要： The present invention relates to pharmaceutical agents useful for therapy and/or prophylaxis in a subject, pharmaceutical composition comprising such compounds, and their use as MCL-1 inhibitors, useful for treating diseases such as cancer.

10. 发明申请

WO2014111457A1 NOVEL SUBSTITUTED PYRIDO-PIPERAZINONE DERIVATIVES AS GAMMA SECRETASE MODULATORS 审中-公开
标题翻译：作为GAMMA秘密调节剂的新型取代的吡咯并吡啶酮衍生物
公开(公告)号：WO2014111457A1
公开(公告)日：2014-07-24
申请号：PCT/EP2014/050787
申请日：2014-01-16
申请人： JANSSEN PHARMACEUTICA NV
发明人： BISCHOFF, François, Paul , VELTER, Adriana, Ingrid , ROMBOUTS, Frederik, Jan, Rita , DE CLEYN, Michel, Anna, Jozef , VAN BRANDT, Sven, Franciscus, Anna , GIJSEN, Henricus, Jacobus, Maria , ZAVATTARO, Chiara , VAN DEN KEYBUS, Frans, Alfons, Maria
IPC分类号： C07D471/04 , A61K31/498 , A61P25/28
CPC分类号： C07D471/04
摘要： The present invention is concerned with novel substituted pyrido-piperazinone derivatives of Formula (I) wherein R 1 , R 2 , R 3 , R 4 , R 5 , L, Z and X have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
摘要翻译：本发明涉及式（I）的新的取代吡啶并哌嗪酮衍生物，其中R 1，R 2，R 3，R 4，R 5，L，Z和X具有权利要求中定义的含义。根据本发明的化合物可用作γ-分泌酶调节剂。本发明还涉及制备这种新化合物的方法，包含所述化合物作为活性成分的药物组合物以及所述化合物作为药物的用途。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式