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公开(公告)号：US10961239B2
公开(公告)日：2021-03-30
申请号：US16475413
申请日：2018-01-03
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： Robert M. Borzilleri , Upender Velaparthi , Chetan Padmakar Darne , Peiying Liu , Manjunatha Narayana Rao Kamble , Balaji Seshadri , Raju Mannoori , Hasibur Rahaman , Jayakumar Sankara Warrier
IPC: C07D487/04 , C07D401/14 , C07D471/04 , A61K45/06 , C07K16/28
Abstract: The invention relates generally to compounds of formula (I) that modulate the activity of TGFβR-1 and TGFβR-2, pharmaceutical compositions containing said compounds and methods of treating proliferative disorders and disorders of dysregulated apoptosis, such as cancer, utilizing the compounds of the invention.
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公开(公告)号：US09242967B2
公开(公告)日：2016-01-26
申请号：US14598721
申请日：2015-01-16
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： Upender Velaparthi , Peiying Liu
IPC: C07D413/00 , C07D333/00 , C07D409/14 , C07D498/04 , C07D413/14 , C07D409/04 , C07D413/04 , C07D487/04 , C07D417/14 , C07D471/04 , C07D495/04 , C07D519/00 , C07D413/06
CPC classification number: C07D498/04 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/06 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D495/04 , C07D519/00
Abstract: Disclosed are azaindazole compounds of Formula (I): or a pharmaceutically acceptable salt thereof, wherein: X is O and Y is N; or X is S and Y is CH; Z is CR2 or N; Q is a heteroaryl; and R1 is defined herein. Also disclosed are methods of using such compounds in the treatment of at least one CYP17 assoC1ated condition, such as, for example, cancer, and pharmaceutical compositions comprising such compounds.
Abstract translation: 公开了式（I）的氮杂吲唑化合物或其药学上可接受的盐，其中：X为O且Y为N; 或X为S，Y为CH; Z是CR2或N; Q是杂芳基; 并且R1在本文中定义。 还公开了使用这些化合物治疗至少一种CYP17相关病症（例如癌症）和包含这些化合物的药物组合物的方法。
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公开(公告)号：US20150126529A1
公开(公告)日：2015-05-07
申请号：US14598721
申请日：2015-01-16
Applicant: Bristol-Myers Squibb Company
Inventor： Upender Velaparthi , Peiying Liu
IPC: C07D409/14 , C07D409/04 , C07D495/04
CPC classification number: C07D498/04 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/06 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D495/04 , C07D519/00
Abstract: Disclosed are azaindazole compounds of Formula (I): or a pharmaceutically acceptable salt thereof, wherein: X is O and Y is N; or X is S and Y is CH; Z is CR2 or N; Q is a heteroaryl; and R1 is defined herein. Also disclosed are methods of using such compounds in the treatment of at least one CYP17 associated condition, such as, for example, cancer, and pharmaceutical compositions comprising such compounds.
Abstract translation: 公开了式（I）的氮杂吲唑化合物或其药学上可接受的盐，其中：X为O且Y为N; 或X为S，Y为CH; Z是CR2或N; Q是杂芳基; 并且R1在本文中定义。 还公开了使用这些化合物治疗至少一种CYP17相关病症例如癌症的方法，以及包含这些化合物的药物组合物。
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公开(公告)号：US09556179B2
公开(公告)日：2017-01-31
申请号：US14653895
申请日：2013-12-20
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： Upender Velaparthi , Chetan Padmakar Darne , Dharmpal S. Dodd , Anthony J. Sampognaro , Mark D. Wittman , Selvakumar Kumaravel , Dibakar Mullick , Peiying Liu , Chandrasekhar Reddy Rachamreddy
IPC: C07D487/04 , C07D519/00
CPC classification number: C07D487/04 , C07D519/00
Abstract: The invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof. The compounds of Formula (I) inhibit protein kinase activity thereby making them useful as anticancer agents.
Abstract translation: 本发明提供式（I）化合物及其药学上可接受的盐。 式（I）的化合物抑制蛋白激酶活性，从而使它们用作抗癌剂。
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公开(公告)号：US20160257690A1
公开(公告)日：2016-09-08
申请号：US15054895
申请日：2016-02-26
Applicant: Rigel Pharmaceuticals, Inc. , Bristol-Myers Squibb Company
Inventor： Todd Kinsella , Marina Gelman , Hui Hong , Ihab S. Darwish , Rajinder Singh , Jiaxin Yu , Robert M. Borzilleri , Upender Velaparthi , Peiying Liu , Chetan Darne , Hasibur Rahaman , Jayakumar Sankara Warrier
IPC: C07D487/04 , C07D471/04
CPC classification number: C07D487/04 , C07D401/04 , C07D403/04 , C07D417/04 , C07D471/04
Abstract: Disclosed are imidazole and thiazole compounds, as well as pharmaceutical compositions and methods of use thereof. One embodiment is a compound having the structure and pharmaceutically acceptable salts, prodrugs and N-oxides thereof (and solvates and hydrates thereof), wherein X, A, Z, R1 and R′ are as described herein. In certain embodiments, a compound disclosed herein inhibits TGF-β, and can be used to treat disease by blocking TGF-β signaling.
Abstract translation: 公开了咪唑和噻唑化合物，以及药物组合物及其使用方法。 一个实施方案是具有其结构和药学上可接受的盐，前药和N-氧化物（及其溶剂化物和水合物）的化合物，其中X，A，Z，R 1和R'如本文所述。 在某些实施方案中，本文公开的化合物抑制TGF-β，并且可用于通过阻断TGF-β信号传导治疗疾病。
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Patent Agency Ranking
![SUBSTITUTED 4,5,6,7-TETRAHYDROPYRAZOLO[1,5-A]PYRAZINE DERIVATIVES AS CASEIN KINASE 1 D/E INHIBITORS](/abs-image/US/2016/10/27/US20160311824A1/abs.jpg.150x150.jpg)
6.发明申请SUBSTITUTED 4,5,6,7-TETRAHYDROPYRAZOLO[1,5-A]PYRAZINE DERIVATIVES AS CASEIN KINASE 1 D/E INHIBITORS 审中-公开取代4,5,6,7-四氢吡唑并[1,5-A]吡啶衍生物作为CASEIN KINASE 1 D / E抑制剂公开(公告)号：US20160311824A1
公开(公告)日：2016-10-27
申请号：US15034217
申请日：2014-11-14
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： Upender Velaparthi , Chetan Padmakar Dame , Peiying Liu , Mark D Wittman , Bradley C. Pearce , Erika M.V. Araujo , Bireshwar Dasgupta , Jalathi Surendran Nair , Sakthi Kumaran Janakiraman , Chandrasekhar Reddy Rachamreddy , Mallikarjuna Rao Mettu , Arul Mozhi Selvan Subbiah Karuppiah , Bandreddy Subba Reddy , Pulicharla Nagalakshmi , Rajesh Onkardas Bora , Shilpa Holehatti Maheshwarappa , Selvakumar Kumaravel , Dibakar Mullick , Ramesh Sistla
IPC: C07D487/04 , C07D487/20 , C07D491/147 , C07D491/20 , C07D519/00 , C07D487/10
CPC classification number: C07D487/04 , C07D487/10 , C07D487/20 , C07D491/147 , C07D491/20 , C07D519/00
Abstract: The invention provides compounds of Formula (I): and pharmaceutically acceptable salts thereof. The compounds of Formula (I) inhibit protein kinase activity thereby making them useful as anticancer agents.
Abstract translation: 及其药学上可接受的盐。 式（I）的化合物抑制蛋白激酶活性，从而使它们用作抗癌剂。
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7.发明授权Pyrazole substituted imidazopyrazines as casein kinase 1 d/e inhibitors 有权吡唑取代的咪唑并吡嗪作为酪蛋白激酶1 d / e抑制剂公开(公告)号：US09475817B2
公开(公告)日：2016-10-25
申请号：US14653878
申请日：2013-12-20
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： Upender Velaparthi , Chetan Padmakar Darne , Dharmpal S. Dodd , Peiying Liu , Christopher P. Mussari , Mark D. Wittman , Selvakumar Kumaravel , Dibakar Mullick
IPC: C07D487/04
CPC classification number: C07D487/04
Abstract: The invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof. The compounds of Formula (I) inhibit protein kinase activity thereby making them useful as anticancer agents.
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公开(公告)号：US20160122358A1
公开(公告)日：2016-05-05
申请号：US14994346
申请日：2016-01-13
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： Upender Velaparthi , Chetan Padmakar Darne , Peiying Liu , Mark D. Wittman , Bradley C. Pearce , Erika M. V. Araujo , Bireshwar Dasgupta , Jalathi Surendran Nair , Sakthi Kumaran Janakiraman , Chandrasekhar Reddy Rachamreddy , Mallikarjuna Rao Mettu , Arul Mozhi Subbiah Karuppiah , Subba Reddy Bandreddy , Nagalakshmi Pulicharla , Rajesh Onkardas Bora , Shilpa Maheshwarappa Holehatti , Selvakumar Kumaravel , Dibakar Mullick , Ramesh Kumar Sistla
IPC: C07D487/04 , C07D487/20 , C07D491/20 , C07D487/10 , C07D491/147
CPC classification number: C07D487/04 , C07D487/10 , C07D487/20 , C07D491/147 , C07D491/20 , C07D519/00
Abstract: The invention provides compounds of Formula (I): and pharmaceutically acceptable salts thereof. The compounds of Formula (I) inhibit protein kinase activity thereby making them useful as anticancer agents.
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9.发明授权公开(公告)号：US09273058B2
公开(公告)日：2016-03-01
申请号：US14541343
申请日：2014-11-14
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： Upender Velaparthi , Chetan Padmakar Darne , Peiying Liu , Mark D. Wittman , Bradley C. Pearce , Erika M. V. Araujo , Bireshwar Dasgupta , Jalathi Surendran Nair , Sakthi Kumaran Janakiraman , Chandrasekhar Reddy Rachamreddy , Mettu Mallikarjuna Rao , Arul Mozhi Selvan Subbiah Karuppiah , Bandreddy Subba Reddy , Pulicharla Nagalakshmi , Rajesh Onkardas Bora , Shilpa Holehatti Maheshwarappa , Selvakumar Kumaravel , Dibakar Mullick , Ramesh Sistla
IPC: C07D487/04 , C07D487/10 , C07D487/20 , C07D491/147 , C07D491/20 , A61K31/4985 , A61K31/499 , A61K31/501 , A61K31/506 , A61K31/5377 , A61P19/02
CPC classification number: C07D487/04 , C07D487/10 , C07D487/20 , C07D491/147 , C07D491/20 , C07D519/00
Abstract: The invention provides compounds of Formula (I): and pharmaceutically acceptable salts thereof. The compounds of Formula (I) inhibit protein kinase activity thereby making them useful as anticancer agents.
Abstract translation: 本发明提供式（I）化合物及其药学上可接受的盐。 式（I）的化合物抑制蛋白激酶活性，从而使它们用作抗癌剂。
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10.发明申请公开(公告)号：US20150344481A1
公开(公告)日：2015-12-03
申请号：US14653895
申请日：2013-12-20
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： Upender Velaparthi , Chetan Padmakar Darne , Dharmpal S. Dodd , Anthony J. Sampognaro , Mark D. Wittman , Selvakumar Kumaravel , Dibakar Mullick , Peiying Liu , Chandrasekhar Reddy Rachamreddy
IPC: C07D487/04 , C07D519/00
CPC classification number: C07D487/04 , C07D519/00
Abstract: The invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof. The compounds of Formula (I) inhibit protein kinase activity thereby making them useful as anticancer agents.
Abstract translation: 本发明提供式（I）化合物及其药学上可接受的盐。 式（I）的化合物抑制蛋白激酶活性，从而使它们用作抗癌剂。
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