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1. 发明申请

WO2020254572A1 EGFR INHIBITORS FOR THE TREATMENT OF CANCER 审中-公开
公开(公告)号：WO2020254572A1
公开(公告)日：2020-12-24
申请号：PCT/EP2020/067093
申请日：2020-06-19
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： DOLENTE, Cosimo , GOERGLER, Annick , HEWINGS, David , JAESCHKE, Georg , KUHN, Bernd , NAGEL, Yvonne, Alice , OBST SANDER, Ulrike , RICCI, Antonio , RUEHER, Daniel , STEINER, Sandra
IPC分类号： C07D487/04 , A61P35/00 , A61K31/496 , A61K31/5377 , A61K31/4709 , A61K31/454 , A61K31/4439
摘要： The application relates to (106) specific heterocyclic compounds comprising a thiazole ring, an indazol ring and a 6,7-dihydro-5H- pyrrolo[l,2-c]imidazole ring system, to pharmaceutical compositions containing them and their medical use. The compounds are described as selective allosteric inhibitors of T790M/L858R, T790M/L858R/ C797S, L858R, L858R/C797S containing EGFR mutants and thus useful for the treatment of cancer, in particular non-small cell lung cancer. (formula)

2. 发明申请

WO2022117487A1 NEW INDAZOLE DERIVATIVES 审中-公开
公开(公告)号：WO2022117487A1
公开(公告)日：2022-06-09
申请号：PCT/EP2021/083301
申请日：2021-11-29
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： DOLENTE, Cosimo , GOERGLER, Annick , HEWINGS, David Stephen , JAESCHKE, Georg , OBST SANDER, Ulrike , RICCI, Antonio
IPC分类号： C07D487/04 , A61K31/427 , A61K31/437 , A61K31/4439 , A61K31/4995 , A61K31/5377 , A61P35/00 , C07D487/08
摘要： The invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1-R4 and A are as defined in the description and in the claims. The compound of formula (I) can be used as a medicament.

3. 发明申请

WO2020254546A1 NEW EGFR INHIBITORS 审中-公开
公开(公告)号：WO2020254546A1
公开(公告)日：2020-12-24
申请号：PCT/EP2020/067055
申请日：2020-06-19
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： DOLENTE, Cosimo , GOERGLER, Annick , HEWINGS, David Stephen , JAESCHKE, Georg , KUHN, Bernd , NAGEL, Yvonne Alice , NORCROSS, Roger David , OBST-SANDER, Christa Ulrike , RICCI, Antonio , RUEHER, Daniel , STEINER, Sandra
IPC分类号： A61P35/00 , C07D417/14 , A61K31/427
摘要： The invention provides novel compounds as described herein, compositions including the compounds and methods of using the compounds.

4. 发明申请

WO2019043217A1 DIHYDROBENZIMIDAZOLONES 审中-公开
公开(公告)号：WO2019043217A1
公开(公告)日：2019-03-07
申请号：PCT/EP2018/073584
申请日：2018-09-03
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： GOERGLER, Annick , NORCROSS, Roger , DEY, Fabian , KUSZNIR, Eric Andre
IPC分类号： C07D401/14 , A61K31/4709 , A61K31/5517 , C07D401/04 , C07D401/12 , C07D235/26 , C07D403/04 , C07D403/06 , C07D403/14 , C07D417/04 , C07D487/04 , C07D495/14 , C07D519/00
CPC分类号： C07D235/26 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/14 , C07D417/04 , C07D487/04 , C07D495/14 , C07D519/00
摘要： The present invention provides compounds which bind to the ubiquitously expressed E3 ligase protein cereblon (CRBN) and alter the substrate specificity of the CRBN E3 ubiquitin ligase complex, resulting in breakdown of intrinsic downstream proteins. Present compounds are thus useful for the treatment of various cancers.

5. 发明申请

WO2019043208A1 DIHYDROQUINOLINONES 审中-公开
公开(公告)号：WO2019043208A1
公开(公告)日：2019-03-07
申请号：PCT/EP2018/073555
申请日：2018-09-03
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： BRITSCHGI, Adrian , DEY, Fabian , GOERGLER, Annick , KUSZNIR, Eric Andre , NORCROSS, Roger , WICHERT, Moreno Attilio
IPC分类号： C07D401/14 , A61K31/4704 , C07D401/04 , C07D487/04 , C07D495/14 , C07D519/00
CPC分类号： C07D401/04 , A61K31/4375 , A61K31/4704 , A61K47/55 , C07D401/14 , C07D487/04 , C07D495/14 , C07D519/00
摘要： The present invention provides compounds which bind to the ubiquitously expressed E3 ligase protein cereblon (CRBN) and alter the substrate specificity of the CRBN E3 ubiquitin ligase complex, resulting in breakdown of intrinsic downstream proteins. Present compounds are thus useful for the treatment of various cancers.

6. 发明申请

WO2022117475A1 NEW INDAZOLE DERIVATIVES 审中-公开
公开(公告)号：WO2022117475A1
公开(公告)日：2022-06-09
申请号：PCT/EP2021/083272
申请日：2021-11-29
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： DOLENTE, Cosimo , GOERGLER, Annick , HEWINGS, David Stephen , JAESCHKE, Georg , OBST SANDER, Ulrike , RICCI, Antonio
IPC分类号： C07D487/04 , A61K31/427 , A61K31/4439 , A61K31/445 , A61K31/5377 , A61P35/00
摘要： The invention provides novel compounds having the general formula (I) or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3 and R4 are as described herein. The compound of formula (I) can be used as a medicament.

7. 发明申请

WO2020254565A1 EGFR INHIBITORS FOR THE TREATMENT OF CANCER 审中-公开
公开(公告)号：WO2020254565A1
公开(公告)日：2020-12-24
申请号：PCT/EP2020/067082
申请日：2020-06-19
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： DOLENTE, Cosimo , GOERGLER, Annick , HEWINGS, David , JAESCHKE, Georg , KUHN, Bernd , NAGEL, Yvonne Alice , OBST SANDER, Ulrike , RICCI, Antonio , RUEHER, Daniel , STEINER, Sandra
IPC分类号： C07D487/04 , A61P35/00 , A61K31/496 , A61K31/5377 , A61K31/4709 , A61K31/454 , A61K31/4439
摘要： The application relates to 17 specific compounds containing a thiazole ring, an indazol ring and a 6,7-dihydro-5H-pyrrolo[l,2-c]imidazole ring system, to pharmaceutical compositions containing them and their medical use. The compounds are described as selective allosteric inhibitors of T790M/L858R, T790M/L858R/C797S, L858R, L858R/C797S containing EGFR mutants and thus useful for the treatment of cancer, in particular non-small cell lung cancer. (Formula)

8. 发明申请

WO2020254562A1 EGFR INHIBITOR FOR THE TREATMENT OF CANCER 审中-公开
公开(公告)号：WO2020254562A1
公开(公告)日：2020-12-24
申请号：PCT/EP2020/067076
申请日：2020-06-19
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： DOLENTE, Cosimo , GOERGLER, Annick , HEWINGS, David , JAESCHKE, Georg , KUHN, Bernd , NAGEL, Yvonne, Alice , OBST SANDER, Ulrike , RICCI, Antonio , RUEHER, Daniel , STEINER, Sandra
IPC分类号： C07D487/04 , A61P35/00 , A61K31/496 , A61K31/5377 , A61K31/4709 , A61K31/454 , A61K31/4439
摘要： The application relates to a compound of formula (I) containing a thiazole ring, an indazol ring and a 6,7-dihydro-5H-pyrrolo[l,2- c]imidazole ring system, to pharmaceutical compositions containing it and its medical use. The compounds are described as selective allosteric inhibitors of T790M/L858R, T790M/L858R/C797S, L858R, L858R/C797S containing EGFR mutants and thus useful for the treatment of cancer, in particular non-small cell lung cancer. (Formula I)

9. 发明申请

WO2019043214A1 GLUTARIMIDE 审中-公开
公开(公告)号：WO2019043214A1
公开(公告)日：2019-03-07
申请号：PCT/EP2018/073578
申请日：2018-09-03
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： GOERGLER, Annick , NORCROSS, Roger , SCHMID, Philipp , DEY, Fabian , KUSZNIR, Eric Andre
IPC分类号： C07D401/12 , A61K31/45 , A61K31/4523 , C07D405/12 , C07D409/12 , C07D487/04 , C07D211/88 , C07D495/14 , C07D519/00
CPC分类号： C07D211/88 , A61K31/4412 , A61K31/4709 , A61K31/498 , A61K47/55 , C07D401/12 , C07D405/12 , C07D409/12 , C07D487/04 , C07D495/14 , C07D519/00
摘要： The present invention provides compounds which bind to the ubiquitously expressed E3 ligase protein cereblon (CRBN) and alter the substrate specificity of the CRBN E3 ubiquitin ligase complex, resulting in breakdown of intrinsic downstream proteins. Present compounds are thus useful for the treatment of various cancers.

10. 发明申请

WO2018087018A1 PHENOXYTRIAZOLES 审中-公开
公开(公告)号：WO2018087018A1
公开(公告)日：2018-05-17
申请号：PCT/EP2017/078260
申请日：2017-11-06
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： BARTELS, Bjoern , BERCHTOLD, Stefan , GALLEY, Guido , GOERGLER, Annick , JAKOB-ROETNE, Roland , KRUMMENACHER, Daniela , LIMBERG, Anja , NEIDHART, Werner , RATNI, Hasane , REUTLINGER, Michael , RODRIGUEZ SARMIENTO, Rosa Maria , SCHNIDER, Christian
IPC分类号： C07D401/14 , C07D413/14 , C07D403/14 , C07D417/14 , A61K31/433 , A61K31/431 , A61K31/4245 , A61K31/435 , A61K31/44 , A61K31/497 , A61P25/00
摘要： The present invention relates to a compound of formula I, HetAr is a five or six membered heteroaryl group, selected from wherein R 1 is hydrogen, halogen, lower alkyl, lower alkoxy or lower alkyl substituted by halogen, and may be the same or different, if two R 1 occur; R 2 is lower alkyl or a mono- or polydeutered derivative thereof, lower alkyl substituted by halogen or lower alkoxy, lower alkenyl unsubstituted or substituted by halogen, cycloalkyl or CH 2 -cycloalkyl unsubstituted or substituted by halogen, heterocycloalkyl or CH 2 -heterocycloalkyl unsubstituted or substituted by lower alkyl; R 3 is halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy substituted by halogen or S(0) 2 -lower alkyl; n is 1, 2 or 3; if n is >1, then R 3 may be the same or different; or to a pharmaceutically active acid addition salt thereof, to a racemic mixture or to its corresponding enantiomer and/or an optical isomer and/or stereoisomer thereof. The compounds may be used for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica or Down syndrome.
摘要翻译：本发明涉及式I化合物，HetAr是五元或六元杂芳基，选自：其中R1是氢，卤素，低级烷基，低级烷氧基或被卤素取代的低级烷基，并且如果两个R 1出现则可以相同或不同; R 2是低级烷基或其单或多缩合衍生物，被卤素或低级烷氧基取代的低级烷基，未被取代或被卤素，环烷基或CH 2 2 - 取代的低级链烯基，未被取代或被低级烷基取代的卤素，杂环烷基或CH 2 - 杂环烷基取代的环烷基; R 3为卤素，低级烷基，被卤素取代的低级烷基，被卤素取代的低级烷氧基或S（O）2 - 低级烷基; n是1,2或3; 如果n> 1，则R 3可以相同或不同; 或其药学活性酸加成盐与外消旋混合物或其相应的对映体和/或其旋光异构体和/或立体异构体反应。这些化合物可用于治疗阿尔茨海默氏病，脑淀粉样血管病，具有淀粉样变性的遗传性脑出血，荷兰型（HCHWA-D），多发梗塞性痴呆，拳击员痴呆或唐氏综合症。

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