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公开(公告)号：US09273014B2
公开(公告)日：2016-03-01
申请号：US14627573
申请日：2015-02-20
Applicant: Bristol-Myers Squibb Company
Inventor： Ashvinikumar V. Gavai , George V. DeLucca , Daniel O'Malley , Patrice Gill , Claude A. Quesnelle , Brian E. Fink , Yufen Zhao , Francis Y. Lee
IPC: A61K38/00 , A61K47/00 , C07D243/24 , A61K31/5513 , A61K31/573 , A61K31/675 , A61K38/05 , A61K45/06 , C07D401/04 , C07F9/645 , C07K5/062 , C07D243/18 , C07D243/26 , C07F9/12 , A61K9/00 , A61K9/08 , A61K31/138 , A61K31/337 , A61K31/506 , A61K31/555 , C07F7/18 , C07F9/38 , A61K9/48 , A61K47/48
CPC classification number: C07D243/24 , A61K9/0019 , A61K9/0095 , A61K9/08 , A61K9/4866 , A61K31/138 , A61K31/337 , A61K31/506 , A61K31/5513 , A61K31/555 , A61K31/573 , A61K31/675 , A61K45/06 , A61K47/64 , C07D243/18 , C07D243/26 , C07D401/04 , C07F7/1804 , C07F9/12 , C07F9/38 , C07F9/645 , A61K2300/00
Abstract: Disclosed are compounds of Formula (I) and/or salts thereof: wherein R1 is —CH2CH2CF3; R2 is —CH2CH2CF3 or —CH2CH2CH2CF3; R3 is H, —CH3, or Rx; R4 is H or Ry; Ring A is phenyl or pyridinyl; and Rx, Ry, Ra, Rb, y, and z are defined herein. Also disclosed are methods of using such compounds to inhibit the Notch receptor, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as cancer; or as prodrugs of such compounds.
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2.发明申请公开(公告)号：US20140087992A1
公开(公告)日：2014-03-27
申请号：US14032333
申请日：2013-09-20
Applicant: Bristol-Myers Squibb Company
Inventor： Ashvinikumar V. Gavai , George V. DeLucca , Daniel O'Malley , Patrice Gill , Claude A. Quesnelle , Brian E. Fink , Yufen Zhao , Francis Y. Lee
IPC: C07D243/24 , A61K45/06 , A61K31/573 , C07K5/062 , A61K31/675 , C07D401/04 , A61K38/05 , A61K31/5513 , C07F9/645
CPC classification number: C07D243/24 , A61K9/0019 , A61K9/0095 , A61K9/08 , A61K9/4866 , A61K31/138 , A61K31/337 , A61K31/506 , A61K31/5513 , A61K31/555 , A61K31/573 , A61K31/675 , A61K45/06 , A61K47/64 , C07D243/18 , C07D243/26 , C07D401/04 , C07F7/1804 , C07F9/12 , C07F9/38 , C07F9/645 , A61K2300/00
Abstract: Disclosed are compounds of Formula (I) and/or salts thereof: wherein R1 is —CH2CH2CF3; R2 is —CH2CH2CF3 or —CH2CH2CH2CF3; R3 is H, —CH3, or Rx; R4 is H or Ry; Ring A is phenyl or pyridinyl; and Rx, Ry, Ra, Rb, y, and z are defined herein. Also disclosed are methods of using such compounds to inhibit the Notch receptor, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as cancer; or as prodrugs of such compounds.
Abstract translation: 公开了式（I）和/或其盐的化合物：其中R 1是-CH 2 CH 2 CF 3; R2是-CH2CH2CF3或-CH2CH2CH2CF3; R3是H，-CH3或Rx; R4是H或Ry; 环A是苯基或吡啶基; 并且Rx，Ry，Ra，Rb，y和z在本文中定义。 还公开了使用这些化合物抑制Notch受体的方法，以及包含这些化合物的药物组合物。 这些化合物可用于治疗，预防或减缓各种治疗领域（例如癌症）中疾病或病症的发展; 或作为这些化合物的前药。
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公开(公告)号：US09133139B2
公开(公告)日：2015-09-15
申请号：US14429941
申请日：2013-09-20
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： Ashvinikumar V. Gavai , Weifang Shan , James Aaron Balog , Claude A. Quesnelle , Wen-Ching Han , George V. DeLucca , Daniel O'Malley , Brian E. Fink
IPC: C07D413/14 , C07D401/04 , C07D401/12 , C07D413/12 , C07D243/24 , A61K31/5513 , C07D491/056 , A61K45/06
CPC classification number: C07D243/24 , A61K31/5513 , A61K45/06 , C07D401/04 , C07D401/12 , C07D413/12 , C07D413/14 , C07D491/04 , C07D491/056
Abstract: Disclosed are compounds of Formula (I): wherein: R2 is phenyl, fluorophenyl, chlorophenyl, trifluorophenyl, methylisoxazolyl, or pyridinyl; R3 is H, CH3, CH2(cyclopropyl), pyridinyl, chloropyridinyl, or methoxypyridinyl: and Ra, Rb, y, and z are defined herein. Also disclosed are methods of using such compounds to inhibit the Notch receptor, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as cancer.
Abstract translation: 公开了式（I）的化合物：其中：R 2是苯基，氟苯基，氯苯基，三氟苯基，甲基异恶唑基或吡啶基; R 3是H，CH 3，CH 2（环丙基），吡啶基，氯吡啶基或甲氧基吡啶基：和R a，R b，y和z在本文中定义。 还公开了使用这些化合物抑制Notch受体的方法，以及包含这些化合物的药物组合物。 这些化合物可用于治疗，预防或减缓各种治疗领域（例如癌症）中疾病或病症的发展。
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Patent Agency Ranking
公开(公告)号：US20150239851A1
公开(公告)日：2015-08-27
申请号：US14429935
申请日：2013-09-20
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： Ashvinikumar V. Gavai , Yufen Zhao , Daniel O'Malley , Claude A. Quesnelle , Brian E. Fink , Derek J. Norris , Wen-Ching Han , George V. DeLucca
IPC: C07D243/24 , A61K45/06 , A61K31/675 , C07D403/12 , A61K31/5513 , C07F9/645
CPC classification number: C07D243/24 , A61K31/5513 , A61K31/675 , A61K45/06 , C07D401/04 , C07D401/12 , C07D403/12 , C07F9/12 , C07F9/645
Abstract: Disclosed are compounds of Formula (I) and/or salts thereof: (I) wherein: R1 is CH2CH2CF3; R2 is CH2(cyclopropyl), CH(CH3)(cyclopropyl), or CH2CH2CH3; R3 is H, CH3, or Rx; R4 is H or Ry; and Rx, Ry, Ra, Rb, Rc, y, and z are defined herein. Also disclosed are methods of using such compounds to inhibit the Notch receptor, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as cancer. The compounds of Formula (I) also include prodrugs of the Notch inhibitor compounds.
Abstract translation: 公开了式（I）和/或其盐的化合物：（I）其中：R 1是CH 2 CH 2 CF 3; R2是CH2（环丙基），CH（CH3）（环丙基）或CH2CH2CH3; R3是H，CH3或Rx; R4是H或Ry; 并且Rx，Ry，Ra，Rb，Rc，y和z在本文中定义。 还公开了使用这些化合物抑制Notch受体的方法，以及包含这些化合物的药物组合物。 这些化合物可用于治疗，预防或减缓各种治疗领域（例如癌症）中疾病或病症的发展。 式（I）的化合物还包括Notch抑制剂化合物的前药。
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5.发明申请公开(公告)号：US20150166489A1
公开(公告)日：2015-06-18
申请号：US14627573
申请日：2015-02-20
Applicant: Bristol-Myers Squibb Company
Inventor： Ashvinikumar V. Gavai , George V. DeLucca , Daniel O'Malley , Patrice Gill , Claude A. Quesnelle , Brian E. Fink , Yufen Zhao , Francis Y. Lee
IPC: C07D243/24 , C07F9/38 , C07K5/062 , C07D401/04
CPC classification number: C07D243/24 , A61K9/0019 , A61K9/0095 , A61K9/08 , A61K9/4866 , A61K31/138 , A61K31/337 , A61K31/506 , A61K31/5513 , A61K31/555 , A61K31/573 , A61K31/675 , A61K45/06 , A61K47/64 , C07D243/18 , C07D243/26 , C07D401/04 , C07F7/1804 , C07F9/12 , C07F9/38 , C07F9/645 , A61K2300/00
Abstract: Disclosed are compounds of Formula (I) and/or salts thereof: wherein R1 is —CH2CH2CF3; R2 is —CH2CH2CF3 or —CH2CH2CH2CF3; R3 is H, —CH3, or Rx; R4 is H or Ry; Ring A is phenyl or pyridinyl; and Rx, Ry, Ra, Rb, y, and z are defined herein. Also disclosed are methods of using such compounds to inhibit the Notch receptor, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as cancer; or as prodrugs of such compounds.
Abstract translation: 公开了式（I）和/或其盐的化合物：其中R 1是-CH 2 CH 2 CF 3; R2是-CH2CH2CF3或-CH2CH2CH2CF3; R3是H，-CH3或Rx; R4是H或Ry; 环A是苯基或吡啶基; 并且Rx，Ry，Ra，Rb，y和z在本文中定义。 还公开了使用这些化合物抑制Notch受体的方法，以及包含这些化合物的药物组合物。 这些化合物可用于治疗，预防或减缓各种治疗领域（例如癌症）中疾病或病症的发展; 或作为这些化合物的前药。
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公开(公告)号：US09242941B2
公开(公告)日：2016-01-26
申请号：US14429935
申请日：2013-09-20
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： Ashvinikumar V. Gavai , Yufen Zhao , Daniel O'Malley , Claude A. Quesnelle , Brian E. Fink , Derek J. Norris , Wen-Ching Han , George V. DeLucca
IPC: C07D401/04 , C07D243/24 , C07F9/12 , C07F9/645 , A61K31/5513 , A61K31/675 , A61K45/06 , C07D403/12
CPC classification number: C07D243/24 , A61K31/5513 , A61K31/675 , A61K45/06 , C07D401/04 , C07D401/12 , C07D403/12 , C07F9/12 , C07F9/645
Abstract: Disclosed are compounds of Formula (I) and/or salts thereof: (I) wherein: R1 is CH2CH2CF3; R2 is CH2(cyclopropyl), CH(CH3)(cyclopropyl), or CH2CH2CH3; R3 is H, CH3, or Rx; R4 is H or Ry; and Rx, Ry, Ra, Rb, Rc, y, and z are defined herein. Also disclosed are methods of using such compounds to inhibit the Notch receptor, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as cancer. The compounds of Formula (I) also include prodrugs of the Notch inhibitor compounds.
Abstract translation: 公开了式（I）和/或其盐的化合物：（I）其中：R 1是CH 2 CH 2 CF 3; R2是CH2（环丙基），CH（CH3）（环丙基）或CH2CH2CH3; R3是H，CH3或Rx; R4是H或Ry; 并且Rx，Ry，Ra，Rb，Rc，y和z在本文中定义。 还公开了使用这些化合物抑制Notch受体的方法，以及包含这些化合物的药物组合物。 这些化合物可用于治疗，预防或减缓各种治疗领域（例如癌症）中疾病或病症的发展。 式（I）的化合物还包括Notch抑制剂化合物的前药。
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公开(公告)号：US20150218111A1
公开(公告)日：2015-08-06
申请号：US14429941
申请日：2013-09-20
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： Ashvinikumar V. Gavai , Weifang Shan , James Aaron Balog , Claude A. Quesnelle , Wen-Ching Han , George V. DeLucca , Daniel O'Malley , Brian E. Fink
IPC: C07D243/24 , C07D413/12 , A61K45/06 , C07D413/14 , C07D401/04 , C07D491/056 , A61K31/5513 , C07D401/12
CPC classification number: C07D243/24 , A61K31/5513 , A61K45/06 , C07D401/04 , C07D401/12 , C07D413/12 , C07D413/14 , C07D491/04 , C07D491/056
Abstract: Disclosed are compounds of Formula (I): wherein: R2 is phenyl, fluorophenyl, chlorophenyl, trifluorophenyl, methylisoxazolyl, or pyridinyl; R3 is H, CH3, CH2(cyclopropyl), pyridinyl, chloropyridinyl, or methoxypyridinyl: and Ra, Rb, y, and z are defined herein. Also disclosed are methods of using such compounds to inhibit the Notch receptor, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as cancer.
Abstract translation: 公开了式（I）的化合物：其中：R 2是苯基，氟苯基，氯苯基，三氟苯基，甲基异恶唑基或吡啶基; R 3是H，CH 3，CH 2（环丙基），吡啶基，氯吡啶基或甲氧基吡啶基：和R a，R b，y和z在本文中定义。 还公开了使用这些化合物抑制Notch受体的方法，以及包含这些化合物的药物组合物。 这些化合物可用于治疗，预防或减缓各种治疗领域（例如癌症）中疾病或病症的发展。
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8.发明授权公开(公告)号：US08999918B2
公开(公告)日：2015-04-07
申请号：US14032333
申请日：2013-09-20
Applicant: Bristol-Myers Squibb Company
Inventor： Ashvinikumar V. Gavai , George V. DeLucca , Daniel O'Malley , Patrice Gill , Claude A. Quesnelle , Brian E. Fink , Yufen Zhao , Francis Y. Lee
IPC: A61K38/00 , A61K47/00 , C07D243/24 , A61K31/5513 , A61K31/573 , A61K31/675 , A61K38/05 , A61K45/06 , C07D401/04 , C07F9/645 , C07K5/062 , C07D243/18 , C07D243/26 , C07F9/12 , A61K9/00 , A61K9/08 , A61K31/138 , A61K31/337 , A61K31/506 , A61K31/555 , A61K9/48 , A61K47/48
CPC classification number: C07D243/24 , A61K9/0019 , A61K9/0095 , A61K9/08 , A61K9/4866 , A61K31/138 , A61K31/337 , A61K31/506 , A61K31/5513 , A61K31/555 , A61K31/573 , A61K31/675 , A61K45/06 , A61K47/64 , C07D243/18 , C07D243/26 , C07D401/04 , C07F7/1804 , C07F9/12 , C07F9/38 , C07F9/645 , A61K2300/00
Abstract: Disclosed are compounds of Formula (I) and/or salts thereof: wherein R1 is —CH2CH2CF3; R2 is —CH2CH2CF3 or —CH2CH2CH2CF3; R3 is H, —CH3, or Rx; R4 is H or Ry; Ring A is phenyl or pyridinyl; and Rx, Ry, Ra, Rb, y, and z are defined herein. Also disclosed are methods of using such compounds to inhibit the Notch receptor, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as cancer; or as prodrugs of such compounds.
Abstract translation: 公开了式（I）和/或其盐的化合物：其中R 1是-CH 2 CH 2 CF 3; R2是-CH2CH2CF3或-CH2CH2CH2CF3; R3是H，-CH3或Rx; R4是H或Ry; 环A是苯基或吡啶基; 并且Rx，Ry，Ra，Rb，y和z在本文中定义。 还公开了使用这些化合物抑制Notch受体的方法，以及包含这些化合物的药物组合物。 这些化合物可用于治疗，预防或减缓各种治疗领域（例如癌症）中的疾病或病症的进展; 或作为这些化合物的前药。
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