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2. 发明专利

IL272681D0 Macrocyclic mcl-1 inhibitors and methods of use 未知
公开(公告)号：IL272681D0
公开(公告)日：2020-03-31
申请号：IL27268120
申请日：2020-02-14
申请人： ABBVIE DEUTSCHLAND , BRAJE WILFRIED , ABBVIE INC , DOHERTY GEORGE , JANTOS KATJA , JI CHENG , JUDD ANDREW , KUNZER AARON , MASTRACCHIO ANTHONY , SONG XIAOHONG , SOUERS ANDREW , SULLIVAN GERARD , TAO ZHI FU , TESKE JESSE , WANG XILU , WENDT MICHAEL , PENNING THOMAS , LAI CHUNQUI , KLING ANDREAS , POHLKI FRAUKE
发明人： BRAJE WILFRIED , DOHERTY GEORGE , JANTOS KATJA , JI CHENG , JUDD ANDREW , KUNZER AARON , MASTRACCHIO ANTHONY , SONG XIAOHONG , SOUERS ANDREW , SULLIVAN GERARD , TAO ZHI-FU , TESKE JESSE , WANG XILU , WENDT MICHAEL , PENNING THOMAS , LAI CHUNQUI , KLING ANDREAS , POHLKI FRAUKE
IPC分类号： C07D20060101
摘要： The present disclosure provides for compounds of formula (I)wherein A 2 , A 3 , A 4 , A 6 , A 7 , A 8 , A 15 , R A , R 5 , R 9 , R 10A , R 10B , R 11 , R 12 , R 13 , R 14 , R 16 , W, X, and Y have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including cancer. Also provided are pharmaceutical compositions comprising compounds of formula (I).

3. 发明专利

SG11202001182QA MACROCYCLIC MCL-1 INHIBITORS AND METHODS OF USE 未知
公开(公告)号：SG11202001182QA
公开(公告)日：2020-03-30
申请号：SG11202001182Q
申请日：2018-08-15
申请人： ABBVIE INC , ABBVIE DEUTSCHLAND , BRAJE WILFRIED , DOHERTY GEORGE , JANTOS KATJA , JI CHENG , JUDD ANDREW , KUNZER AARON , MASTRACCHIO ANTHONY , SONG XIAOHONG , SOUERS ANDREW , SULLIVAN GERARD , TAO ZHI FU , TESKE JESSE , WANG XILU , WENDT MICHAEL , PENNING THOMAS , LAI CHUNQUI , KLING ANDREAS , POHLKI FRAUKE
发明人： BRAJE WILFRIED , DOHERTY GEORGE , JANTOS KATJA , JI CHENG , JUDD ANDREW , KUNZER AARON , MASTRACCHIO ANTHONY , SONG XIAOHONG , SOUERS ANDREW , SULLIVAN GERARD , TAO ZHI-FU , TESKE JESSE , WANG XILU , WENDT MICHAEL , PENNING THOMAS , LAI CHUNQUI , KLING ANDREAS , POHLKI FRAUKE
IPC分类号： A61K31/395 , A61P35/00 , C07D515/22
摘要： The present disclosure provides for compounds of formula (I)wherein A 2 , A 3 , A 4 , A 6 , A 7 , A 8 , A 15 , R A , R 5 , R 9 , R 10A , R 10B , R 11 , R 12 , R 13 , R 14 , R 16 , W, X, and Y have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including cancer. Also provided are pharmaceutical compositions comprising compounds of formula (I).

4. 发明申请

WO2019035911A1 MACROCYCLIC MCL-1 INHIBITORS AND METHODS OF USE 审中-公开
公开(公告)号：WO2019035911A1
公开(公告)日：2019-02-21
申请号：PCT/US2018/000180
申请日：2018-08-15
申请人： ABBVIE INC. , ABBVIE DEUTSCHLAND GMBH & CO. KG , BRAJE, Wilfried , DOHERTY, George , JANTOS, Katja , JI, Cheng , JUDD, Andrew , KUNZER, Aaron , MASTRACCHIO, Anthony , SONG, Xiaohong , SOUERS, Andrew , SULLIVAN, Gerard , TAO, Zhi-Fu , TESKE, Jesse , WANG, Xilu , WENDT, Michael , PENNING, Thomas , LAI, Chunqui , KLING, Andreas , POHLKI, Frauke
发明人： BRAJE, Wilfried , DOHERTY, George , JANTOS, Katja , JI, Cheng , JUDD, Andrew , KUNZER, Aaron , MASTRACCHIO, Anthony , SONG, Xiaohong , SOUERS, Andrew , SULLIVAN, Gerard , TAO, Zhi-Fu , TESKE, Jesse , WANG, Xilu , WENDT, Michael , PENNING, Thomas , LAI, Chunqui , KLING, Andreas , POHLKI, Frauke
IPC分类号： A61K31/395 , A61P35/00 , C07D515/22
摘要： The present disclosure provides for compounds of formula (I), wherein A 2 , A 3 , A 4 , A 6 , A 7 , A 8 , A 15 , R A , R 5 , R 9 , R 10A , R 10B , R 11 , R 12 , R 13 , R 14 , R 16 , W, X, and Y have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including cancer. Also provided are pharmaceutical compositions comprising compounds of formula (I).

5. 发明申请

WO2012076639A1 CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS V 审中-公开
标题翻译：羧酰胺化合物及其作为钙抑制剂V
公开(公告)号：WO2012076639A1
公开(公告)日：2012-06-14
申请号：PCT/EP2011/072164
申请日：2011-12-08
申请人： ABBOTT GMBH & CO. KG , ABBOTT LABORATORIES , KLING, Andreas , JANTOS, Katja , MACK, Helmut , MÖLLER, Achim , HORNBERGER, Wilfried , LAO, Yanbin , BACKFISCH, Gisela , NIJSEN, Marjoleen
发明人： KLING, Andreas , JANTOS, Katja , MACK, Helmut , MÖLLER, Achim , HORNBERGER, Wilfried , LAO, Yanbin , BACKFISCH, Gisela , NIJSEN, Marjoleen
IPC分类号： A61K31/4439 , C07D401/04 , A61P25/28
CPC分类号： C07D401/04 , A61K31/4439 , C07D401/14 , Y02A50/411
摘要： The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula (I) in which R 1 , R 2 , R 3 R 4 , X, m and n have the meanings mentioned in the claims and the description, the tautomers thereof, the hydrates thereof and the pharmaceutically suitable salts thereof. Of these compounds those are preferred wherein R 1 is optionally substituted benzyl or hetaryl-methyl, X is a single bond or an oxygen atom, R 2 is C 1 -C 4 - alkyl, C 1 -C 4 -haloalkyl, C 2 -C 4 -alkenyl, C 3 -C 6 -cycloalkyl, C 3 -C 6 -cycloalkyl-C 1 -C 2 -alkyl, C 3 -C 6 -heterocycloalkyl-C 1 -C 2 -alkyl, phenyl, phenyl-C 1 -C 3 -alkyl, pyridin-2-yl-C 1 -C 3 -alkyl or CH 2 -C(O)OCH 3 ,R 3 and R 4 independently of one another are halogen, CN, CF 3 , CHF 2 , CH 2 F, C 1 -C 2 -alkyl or C 1 -C 2 -alkoxy, and m and n independently of one another are 0 or 1.
摘要翻译：本发明涉及新的羧酰胺化合物及其用于制备药物的用途。羧酰胺化合物是钙蛋白酶（钙依赖性半胱氨酸蛋白酶）的抑制剂。因此，本发明还涉及这些羧酰胺化合物用于治疗与升高的钙蛋白酶活性相关的病症的用途。羧酰胺化合物是通式（I）的化合物，其中R 1，R 2，R 3，R 4，X，m和n具有权利要求书和描述中所述的含义，其互变异构体，其水合物及其药学上合适的盐。在这些化合物中，优选其中R 1为任选取代的苄基或杂芳基 - 甲基，X为单键或氧原子，R 2为C 1 -C 4烷基，C 1 -C 4卤代烷基，C 2 -C 4 - 烯基，C 3 -C 6 环烷基，C 3 -C 6 - 环烷基-C 1 -C 2 - 烷基，C 3 -C 6 - 杂环烷基-C 1 -C 2烷基，苯基，苯基-C 1 -C 3 - 烷基，吡啶-2-基-C 1 -C 3 - 烷基或CH 2 -C（O）OCH 3，R 3和R 4彼此独立地是卤素，CN，CF 3，CHF 2，CH 2 F，C 1 -C 2 - 烷基或C 1 -C 2 - 烷氧基，m和n彼此独立地为0或1。

6. 发明申请

WO2011076812A1 CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS IV 审中-公开
标题翻译：羧酰胺化合物及其作为抑制剂的用途IV
公开(公告)号：WO2011076812A1
公开(公告)日：2011-06-30
申请号：PCT/EP2010/070420
申请日：2010-12-21
申请人： ABBOTT GMBH & CO. KG , ABBOTT LABORATORIES , KLING, Andreas , JANTOS, Katja , MACK, Helmut , MÖLLER, Achim , HORNBERGER, Wilfried , BACKFISCH, Gisela , LAO, Yanbin , NIJSEN, Marjoleen
发明人： KLING, Andreas , JANTOS, Katja , MACK, Helmut , MÖLLER, Achim , HORNBERGER, Wilfried , BACKFISCH, Gisela , LAO, Yanbin , NIJSEN, Marjoleen
IPC分类号： C07D401/04 , A61K31/4439 , A61P25/00
CPC分类号： C07D401/04 , C07D401/14 , C07D413/14
摘要： The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula I in which R 1 , R 2 , R 3 R 4 , R 5 ,, m and n have the meanings mentioned in the claims and the description, the tautomers thereof, the hydrates thereof and the pharmaceutically suitable salts thereof. Of these compounds those are preferred wherein R 1 is optionally substituted phenyl-C 1 -C 2 -alkyl or hetaryl-C 1 -C 2 -alkyl, R 2 is optionally substituted aryl, hetaryl, aryl-C 1 -C 6 -alkyl, aryl-C 2 -C 6 -alkenyl or hetaryl-C 1 -C 4 -alkyl, R 3 is C 3 -C 4 -alkyl, C 1 -C 4 -haloalkyl, C 2 -C 4 -alkenyl, C 3 -C 6 -cycloalkyl, C 3 -C 6 -cycloalkyl-C 1 -C 2 -alkyl, C 3 -C 6 - heterocycloalkyl-C 1 -C 2 -alkyl, phenyl-C 1 -C 3 -alkyl, pyridin-2-yl-C 1 -C 3 -alkyl or 1,3- benzoxazol-2-yl-methyl, R 4 and R 5 independently of one another are halogen, CF 3 , CHF 2 , CH 2 F, C 1 -C 2 -alkyl or C 1 -C 2 -alkoxy, and m and n independently of one another are 0 or 1.
摘要翻译：本发明涉及新的羧酰胺化合物及其用于制备药物的用途。羧酰胺化合物是钙蛋白酶（钙依赖性半胱氨酸蛋白酶）的抑制剂。因此，本发明还涉及这些羧酰胺化合物用于治疗与升高的钙蛋白酶活性相关的病症的用途。羧酰胺化合物是通式I的化合物，其中R 1，R 2，R 3，R 4，R 5，m和n具有权利要求书和说明书中所述的含义，其互变异构体，其水合物及其药学上合适的盐。在这些化合物中，优选其中R 1为任选取代的苯基-C 1 -C 2 - 烷基或杂芳基-C 1 -C 2烷基，R 2为任选取代的芳基，杂芳基，芳基-C 1 -C 6 - 烷基，芳基-C 2 -C 6 - 烯基或杂芳基-C 1 -C 4 - 烷基，R 3是C 3 -C 4 - 烷基，C 1 -C 4 - 卤代烷基，C 2 -C 4 - 烯基，C 3 -C 6 - 环烷基，C 3 -C 6 - 环烷基-C 1 -C 2烷基，C 3 -C 6 - 杂环烷基-C 1 -C 2 - 烷基，苯基-C 1 -C 3 - 烷基，吡啶-2-基-C1-C3-烷基或1,3-苯并恶唑-2-基 - 甲基，R4和R5彼此独立地是卤素，CF 3，CHF 2，CH 2 F，C 1 -C 2烷基或C 1 -C 2烷氧基，m和n彼此独立地为0或1。

7. 发明申请

WO2019035899A1 MACROCYCLIC MCL-1 INHIBITORS AND METHODS OF USE 审中-公开
公开(公告)号：WO2019035899A1
公开(公告)日：2019-02-21
申请号：PCT/US2018/000167
申请日：2018-08-15
申请人： ABBVIE INC. , ABBVIE DEUTSCHLAND GMBH & CO. KG , BRADY, Patrick , BRAJE, Wilfried , DAI, Yujia , DOHERTY, George , GONG, Jane , JANTOS, Katja , JI, Cheng , JUDD, Andrew , KUNZER, Aaron , MASTRACCHIO, Anthony , RISI, Roberto , SONG, Xiaohong , SOUERS, Andrew , SULLIVAN, Gerard , TAO, Zhi-fu , TESKE, Jesse , WANG, Xilu , WENDT, Michael , YU, Yiyun , ZHU, Guidong , PENNING, Thomas , LAI, Chunqiu
发明人： BRADY, Patrick , BRAJE, Wilfried , DAI, Yujia , DOHERTY, George , GONG, Jane , JANTOS, Katja , JI, Cheng , JUDD, Andrew , KUNZER, Aaron , MASTRACCHIO, Anthony , RISI, Roberto , SONG, Xiaohong , SOUERS, Andrew , SULLIVAN, Gerard , TAO, Zhi-fu , TESKE, Jesse , WANG, Xilu , WENDT, Michael , YU, Yiyun , ZHU, Guidong , PENNING, Thomas , LAI, Chunqiu
IPC分类号： A61K31/395 , A61P35/00 , C07D515/22
摘要： The present disclosure provides for compounds of Formula (I) wherein A 2 , A 3 , A 4 , A 6 , A 7 , A 8 , A 15 , R A , R 5 , R 9 , R 10A , R 10B , R 11 , R 12 , R 13 , R 14 , R 16 , W, X, and Y have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents for the treatment of diseases and conditions, including cancer. Also provided are pharmaceutical compositions comprising compounds of Formula (I).

8. 发明申请

WO2019035927A1 MACROCYCLIC MCL-1 INHIBITORS AND METHODS OF USE 审中-公开
公开(公告)号：WO2019035927A1
公开(公告)日：2019-02-21
申请号：PCT/US2018/000196
申请日：2018-08-15
申请人： ABBVIE INC. , ABBVIE DEUTSCHLAND GMBH & CO. KG , BRAJE, Wilfried , DOHERTY, George , JANTOS, Katja , JI, Cheng , JUDD, Andrew , KUNZER, Aaron , MASTRACCHIO, Anthony , SONG, Xiaohong , SOUERS, Andrew , SULLIVAN, Gerard , TAO, Zhi-Fu , LAI, Chunqui , KLING, Andreas , POHLKI, Frauke , TESKE, Jessc , WENDT, Michael , BRADY, Patrick , WANG, Xilu , PENNING, Thomas , MICHAELIDES, Michael
发明人： BRAJE, Wilfried , DOHERTY, George , JANTOS, Katja , JI, Cheng , JUDD, Andrew , KUNZER, Aaron , MASTRACCHIO, Anthony , SONG, Xiaohong , SOUERS, Andrew , SULLIVAN, Gerard , TAO, Zhi-Fu , LAI, Chunqui , KLING, Andreas , POHLKI, Frauke , TESKE, Jessc , WENDT, Michael , BRADY, Patrick , WANG, Xilu , PENNING, Thomas , MICHAELIDES, Michael
IPC分类号： A61K31/395 , A61P35/00 , C07D515/22
摘要： The present disclosure provides for compounds of Formula (I) wherein A 2 , A 3 , A 4 , A 6 , A 7 , A 8 , A 15 , R A , R 5 , R 9 , R 10A , R 10B , R 11 , R 12 , R 13 , R 14 , R 16 , W, X, and Y have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including cancer. Also provided are pharmaceutical compositions comprising compounds of Formula (I).

9. 发明申请

WO2010128102A1 CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS 审中-公开
标题翻译：羧酰胺化合物及其作为钙蛋白酶抑制剂的用途
公开(公告)号：WO2010128102A1
公开(公告)日：2010-11-11
申请号：PCT/EP2010/056166
申请日：2010-05-06
申请人： ABBOTT GMBH & CO. KG , MACK, Helmut , KLING, Andreas , JANTOS, Katja , MOELLER, Achim , HORNBERGER, Wilfried , HUTCHINS, Charles, W.
发明人： MACK, Helmut , KLING, Andreas , JANTOS, Katja , MOELLER, Achim , HORNBERGER, Wilfried , HUTCHINS, Charles, W.
IPC分类号： C07D207/26 , C07D211/76 , C07D233/34 , C07D239/10 , A61K31/4412
CPC分类号： C07D207/22 , C07D207/26 , C07D207/28 , C07D211/76 , C07D211/78 , C07D213/81 , C07D233/32 , C07D233/34 , C07D239/10 , C07D275/03 , C07D401/06 , C07D401/12 , C07D405/12 , C07D409/12 , C07D417/12
摘要： The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula (I) in which R 1 , R 2 , R 3a , R 3b , R 4 , Q, Y, A and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula (Ia) and (Ib) in which R 1 , r, R 2b , R 3a , R 3b , R 4 , Y and X have the meanings mentioned in the claims, including the tautomers thereof and the pharmaceutically suitable salts thereof. Of these compounds those are preferred wherein Y is a moiety CH 2 -CH 2 , CH 2 -CH 2 -CH 2 , N(R y# )-CH2, N(R y# )-CH 2 -CH 2 or CH=CH-CH=, each optionally having 1 or 2 H-atoms replaced with identical or different radicals R y , wherein R y and R y# have the meanings mentioned in the claims.
摘要翻译：本发明涉及新的羧酰胺化合物及其用于制备药物的用途。羧酰胺化合物是钙蛋白酶（钙依赖性半胱氨酸蛋白酶）的抑制剂。因此，本发明还涉及这些羧酰胺化合物用于治疗与升高的钙蛋白酶活性相关的病症的用途。羧酰胺化合物是通式（I）的化合物，其中R 1，R 2，R 3a，R 3b，R 4，Q，Y，A和X具有权利要求书和描述中所述的含义，其互变异构体和药学上合适的盐它们。特别地，化合物具有通式（Ia）和（Ib），其中R1，r，R2b，R3a，R3b，R4，Y和X具有权利要求中提及的含义，包括其互变异构体和药学上合适的盐它们。在这些化合物中，优选其中Y为CH2-CH2，CH2-CH2-CH2，N（Ry＃）-CH2，N（Ry＃）-CH2-CH2或CH = CH-CH =，各自任选具有1 或2个H原子被相同或不同的基团Ry取代，其中Ry和Ry＃具有权利要求中提及的含义。

10. 发明申请

WO2019035914A1 MACROCYCLIC MCL-1 INHIBITORS AND METHODS OF USE 审中-公开
公开(公告)号：WO2019035914A1
公开(公告)日：2019-02-21
申请号：PCT/US2018/000183
申请日：2018-08-15
申请人： ABBVIE INC. , ABBVIE DEUTSCHLAND GMBH & CO. KG , BRADY, Patrick , BRAJE, Wilfried , DAI, Yujia , DOHERTY, George , GONG, Jane , JANTOS, Katja , JI, Cheng , JUDD, Andrew , KUNZER, Aaron , MASTRACCHIO, Anthony , RISI, Roberto , SONG, Xiaohong , SOUERS, Andrew , SULLIVAN, Gerard , TAO, Zhi-Fu , TESKE, Jesse , WANG, Xilu , WENDT, Michael , YU, Yiyun , ZHU, Guidong , PENNING, Thomas , LAI, Chunqui , KLING, Andreas , POHLKI, Frauke , POTIN, Dominique , GUILLIER, Fabrice
发明人： BRADY, Patrick , BRAJE, Wilfried , DAI, Yujia , DOHERTY, George , GONG, Jane , JANTOS, Katja , JI, Cheng , JUDD, Andrew , KUNZER, Aaron , MASTRACCHIO, Anthony , RISI, Roberto , SONG, Xiaohong , SOUERS, Andrew , SULLIVAN, Gerard , TAO, Zhi-Fu , TESKE, Jesse , WANG, Xilu , WENDT, Michael , YU, Yiyun , ZHU, Guidong , PENNING, Thomas , LAI, Chunqui , KLING, Andreas , POHLKI, Frauke , POTIN, Dominique , GUILLIER, Fabrice
IPC分类号： A61K31/395 , A61P35/00 , C07D515/22
摘要： The present disclosure provides for compounds of Formula (I) wherein A 2 , A 3 , A 4 , A 6 , A 7 , A 8 , A 15 , R A , R 5 , R 9 , R 10A , R 10B , R 11 , R 12 , R 13 , R 14 , R 16 , W, X, and Y have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents for the treatment of diseases and conditions, including cancer. Also provided are pharmaceutical compositions comprising compounds of Formula (I).

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