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1. 发明公开

US20230399340A1 MACROCYCLIC MCL-1 INHIBITORS AND METHODS OF USE 审中-公开
公开(公告)号：US20230399340A1
公开(公告)日：2023-12-14
申请号：US18046011
申请日：2022-10-12
申请人： AbbVie Inc. , AbbVie Deutschland GmbH & Co. KG
发明人： Wilfried Braje , George Doherty , Katja Jantos , Cheng Ji , Andrew Judd , Aaron Kunzer , Anthony Mastracchio , Xiaohong Song , Andrew Souers , Gerard Sullivan , Zhi-Fu Tao , Chunqiu Lai , Andreas Kling , Frauke Pohlki , Jesse Teske , Michael Wendt , Patrick Brady , Xilu Wang , Thomas Penning , Michael Michaelides
IPC分类号： C07D495/16 , A61P35/00 , C07D519/00
CPC分类号： C07D495/16 , A61P35/00 , C07D519/00
摘要： The present disclosure provides for compounds of Formula (I)

wherein A2, A3, A4, A6, A7, A8, A15, RA, R5, R9, R10A, R10B, R11, R12, R13, R14, R16, 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).

2. 发明公开

US20230183261A1 Macrocyclic MCL-1 Inhibitors and Methods of Use 审中-公开
公开(公告)号：US20230183261A1
公开(公告)日：2023-06-15
申请号：US17649906
申请日：2022-02-03
申请人： AbbVie Inc. , AbbVie Deutschland GmbH & Co. KG
发明人： Andrew S. Judd , Aaron R. Kunzer , Chunqiu Lai , Andrew J. Souers , Gerard M. Sullivan , Zhi-Fu Tao , Jesse A. Teske , Anthony Mastracchio , Xilu Wang , Cheng Ji , Michael D. Wendt , Xiaohong Song , George A. Doherty , Katja Jantos , Wilfried Braje , Andreas Kling , Frauke Pohlki , Thomas D. Penning
IPC分类号： C07D495/16 , C07D495/18 , A61K45/06 , C07D495/22 , C07D491/18 , A61K31/519 , C07D491/22 , A61P35/00 , A61P35/02
CPC分类号： C07D495/16 , C07D495/18 , A61K45/06 , C07D495/22 , C07D491/18 , A61K31/519 , C07D491/22 , A61P35/00 , A61P35/02
摘要： The present disclosure provides for compounds of formula (I)

wherein A2, A3, A4, A6, A7, A8, A15, RA, R5, R9, R10A, R10B, R11, R12, R13, R14, R16, 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. 发明授权

US09862704B2 Oxindole derivatives carrying an amine-substituted piperidyl-acetidinyl substituent and use thereof for treating vasopressine-related diseases 有权
公开(公告)号：US09862704B2
公开(公告)日：2018-01-09
申请号：US15106662
申请日：2014-12-19
申请人： AbbVie Deutschland GmbH & Co. KG , AbbVie Inc.
发明人： Hervé Geneste , Wilfried Hornberger , Charles W. Hutchins , Katja Jantos , Andreas Kling , Loic Laplanche , Marcel Van Gaalen
IPC分类号： C07D401/14
CPC分类号： C07D401/14
摘要： The present invention relates to novel substituted oxindole derivatives of formula (I) wherein the variables are as defined in the claims and description; to pharmaceutical compositions comprising them, and to their use for the treatment of vasopressin-related disorders.

4. 发明授权

US09567325B2 Carboxamide compounds and their use as calpain inhibitors 有权
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：US09567325B2
公开(公告)日：2017-02-14
申请号：US14522454
申请日：2014-10-23
申请人： AbbVie Deutschland GmbH & Co. KG , AbbVie Inc.
发明人： Andreas Kling , Helmut Mack , Katja Jantos , Achim Moeller , Wilfried Hornberger , Charles W. Hutchins
IPC分类号： C07D277/30 , C07D417/04 , C07D413/04 , C07D401/04
CPC分类号： C07D417/04 , C07D277/30 , C07D401/04 , C07D413/04
摘要： The present invention relates to novel carboxamide compounds and their use as 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 and to a method for the therapeutic and/or prophylactic treatment by administering an effective amount of at least one of these carboxamide compounds.The carboxamide compounds are compounds of the general formula I in which W—R2 is selected from and R1, R2, R3a, R3b, Y1, Y2, Y3, Y4, X, Q, m, k, Rw and Rw* have the meanings mentioned in the claims, the tautomers thereof and the pharmaceutically suitable salts thereof. Of these compounds those are preferred wherein Y1, Y2, Y3 and Y4 are CRy, or one or two of the variables Y1 to Y4 are a nitrogen atom and the remaining variables are CRy, wherein the radicals Ry may be identical or different and 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作为药物的用途。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钙蛋白酶活性升高相关的疾病的用途，以及通过施用有效量的这些羧酰胺化合物中的至少一种来进行治疗和/或预防性治疗的方法。羧酰胺化合物是其中W-R2选自并且R 1，R 2，R 3a，R 3b，Y 1，Y 2，Y 3，Y 4，X，Q，m，k，Rw和Rw *具有通式I的化合物权利要求中提及的其互变异构体及其药学上合适的盐。在这些化合物中，优选其中Y1，Y2，Y3和Y4为CRy，或变量Y1至Y4中的一个或两个为氮原子，剩余的变量为CRy，其中基团Ry可以相同或不同，并且具有意思是在权利要求中提及。

5. 发明申请

US20150099786A1 CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS 有权
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：US20150099786A1
公开(公告)日：2015-04-09
申请号：US14570996
申请日：2014-12-15
申请人： AbbVie Deutschland GmbH & Co. KG , AbbVie Inc.
发明人： Helmut Mack , Andreas Kling , Katja Jantos , Achim Moeller , Wilfried Hornberger , Charles W. Hutchins
IPC分类号： C07D417/12 , C07D213/81 , C07D401/06 , C07D211/78 , C07D233/32 , C07D401/12 , C07D207/28 , C07D275/03
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 R1, R2, R3a, R3b, R4, 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 R1, r, R2b, R3a, R3b, R4, 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 CH2—CH2, CH2—CH2—CH2, N(Ry#)—CH2, N(Ry#)—CH2—CH2 or CH═CH—CH═, each optionally having 1 or 2 H-atoms replaced with identical or different radicals Ry, wherein Ry and Ry# 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具有权利要求和说明书中所述的含义及其互变异构体及其药学上合适的盐。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，包括其互变异构体及其药学上合适的盐。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。

6. 发明申请

US20140179702A1 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：US20140179702A1
公开(公告)日：2014-06-26
申请号：US14054460
申请日：2013-10-15
申请人： ABBVIE INC. , ABBVIE DEUTSCHLAND GMBH & CO. KG
发明人： Andreas Kling , Katja Jantos , Helmut Mack , Achim Möller , Wilfried Hornberger , Gisela Backfisch , Yanbin Lao , Marjoleen Nijsen
IPC分类号： C07D401/04 , C07D413/14 , C07D401/14
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.
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。

7. 发明申请

US20200325153A1 Macrocyclic MCL-1 Inhibitors and Methods of Use 审中-公开
公开(公告)号：US20200325153A1
公开(公告)日：2020-10-15
申请号：US16872279
申请日：2020-05-11
申请人： AbbVie Inc. , AbbVie Deutschland GmbH & Co. KG
发明人： Andrew S. Judd , Aaron R. Kunzer , Chunqiu Lai , Andrew J. Souers , Gerard M. Sullivan , Zhi-Fu Tao , Jesse A. Teske , Anthony Mastracchio , Xilu Wang , Cheng Ji , Michael D. Wendt , Xiaohong Song , George A. Doherty , Katja Jantos , Wilfried Braje , Andreas Kling , Frauke Pohlki , Thomas D. Penning
IPC分类号： C07D495/16 , C07D495/18 , A61K45/06 , C07D495/22 , C07D491/18 , A61K31/519 , C07D491/22 , A61P35/00 , A61P35/02
摘要： The present disclosure provides for compounds of formula (I) wherein A2, A3, A4, A6, A7, A8, A15, RA, R5, R9, R10A, R10B, R11, R12, R13, R14, R16, 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).

8. 发明申请

US20190144465A1 Macrocyclic MCL-1 inhibitors and methods of use 审中-公开
公开(公告)号：US20190144465A1
公开(公告)日：2019-05-16
申请号：US15998789
申请日：2018-08-15
申请人： AbbVie Inc. , AbbVie Deutschland GmbH & Co. KG
发明人： Andrew S. Judd , Aaron R. Kunzer , Chunqiu Lai , Andrew J. Souers , Gerard M. Sullivan , Zhi-Fu Tao , Jesse A. Teske , Anthony Mastracchio , Xilu Wang , Cheng Ji , Michael D. Wendt , Xiaohong Song , George A. Doherty , Katja Jantos , Wilfried Braje , Andreas Kling , Frauke Pohlki , Thomas D. Penning
IPC分类号： C07D495/16 , A61P35/02
摘要： The present disclosure provides for compounds of formula (I) wherein A2, A3, A4, A6, A7, A8, R15, RA, R5, R9, R10A, R10B, R11, R12, R13, R14, R16, 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. 发明授权

US09840495B2 Oxindole derivatives carrying a piperidyl-substituted azetidinyl substituent and use thereof for treating vasopressine-related diseases 有权
公开(公告)号：US09840495B2
公开(公告)日：2017-12-12
申请号：US15106670
申请日：2014-12-19
申请人： AbbVie Deutschland GmbH & Co. KG , AbbVie Inc.
发明人： Hervé Geneste , Wilfried Hornberger , Charles W. Hutchins , Katja Jantos , Andreas Kling , Loic Laplanche , Marcel Van Gaalen
IPC分类号： A01N43/00 , A61K31/00 , C07D401/14 , C07D401/04 , C07B59/00 , C07D405/14 , C07D491/107
CPC分类号： C07D401/14 , C07B59/002 , C07B2200/05 , C07D401/04 , C07D405/14 , C07D491/107
摘要： The present invention relates to novel substituted oxindole derivatives of formula (I) wherein the variables are as defined in the claims and description; to pharmaceutical compositions comprising them, and to their use for treatment of vasopressin-related disorders.

10. 发明授权

US09527811B2 Carboxamide compounds and their use as calpain inhibitors 有权
公开(公告)号：US09527811B2
公开(公告)日：2016-12-27
申请号：US14570996
申请日：2014-12-15
申请人： AbbVie Deutschland GmbH & Co. KG , AbbVie Inc.
发明人： Helmut Mack , Andreas Kling , Katja Jantos , Achim Moeller , Wilfried Hornberger , Charles W. Hutchins
IPC分类号： C07D207/26 , C07D207/28 , C07D401/12 , C07D233/34 , C07D239/10 , C07D207/22 , C07D211/78 , C07D211/76 , C07D233/32 , C07D275/03 , C07D401/06 , C07D405/12 , C07D409/12 , C07D417/12 , C07D213/81
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 R1, R2, R3a, R3b, R4, 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 R1, r, R2b, R3a, R3b, R4, 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 CH2—CH2, CH2—CH2—CH2, N(Ry#)—CH2, N(Ry#)—CH2—CH2 or CH═CH—CH═, each optionally having 1 or 2H-atoms replaced with identical or different radicals Ry, wherein Ry and Ry# have the meanings mentioned in the claims.

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