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1. 发明申请

WO2013106614A1 TRIAZOLYL-SUBSTITUTED PYRIDYL COMPOUNDS USEFUL AS KINASE INHIBITORS 审中-公开
标题翻译：三唑基取代的吡啶化合物作为激酶抑制剂有用
公开(公告)号：WO2013106614A1
公开(公告)日：2013-07-18
申请号：PCT/US2013/021096
申请日：2013-01-11
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： DODD, Dharmpal, S. , MUSSARI, Christopher, P. , BHIDE, Rajeev, S. , NAIR, Satheesh Kesavan , PAIDI, Venkatram Reddy , KUMAR, Sreekantha Ratna , BANERJEE, Abhisek , SISTLA, Ramesh , PITTS, William, J. , HYNES, John
IPC分类号： C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14 , C07D471/04 , C07D487/04 , A61K31/437 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/496 , A61K31/497 , A61K31/498 , A61K31/5025 , A61K31/506
CPC分类号： C07D471/10 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14 , C07D471/04 , C07D487/04
摘要： Compounds having the following formula:(I) wherein:A is an optionally substiuted triazole, or a stereoisomer or a pharmaceutically-acceptable salt thereof, are useful as kinase modulators, including IRAK-4 modulation.
摘要翻译：具有下式的化合物：（I）其中：A是任选取代的三唑或其立体异构体或其药学上可接受的盐，可用作激酶调节剂，包括IRAK-4调节。

2. 发明申请

WO2021163254A1 HETEROCYCLIC PAD4 INHIBITORS 审中-公开
公开(公告)号：WO2021163254A1
公开(公告)日：2021-08-19
申请号：PCT/US2021/017554
申请日：2021-02-11
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： SELVAKUMAR, Kumaravel , PAIDI, Venkatram Reddy , THANGATHIRUPATHY, Srinivasan , KUMAR CM, Vijaya , ALAJANGI, Tirupathi, Rao , SURA, Mallikarjun, Reddy , MAHADEVU, Krishna , SISTLA, Ramesh, Kumar , AGARWAL, Piyush , SUBBIAH KARUPPIAH, Arul, Mozhi , NAIR, Jalathi, S. , MORAMPUDI, Ooha , PANDA, Manoranjan , TINO, Joseph, A. , CHERNEY, Robert, J. , DUNCIA, John, V. , GARDNER, Daniel, S. , DHAR, T., G., Murali , ROSS, Audrey, Graham , GORMISKY, Paul, E. , ZHU, Xiao , SELETSKY, Boris, M. , ANTROPOW, Alyssa, H. , NIU, Deqiang , ZHU, Zhengdong , MIAO, Guobin , CUERVO, Julio, Hernán
IPC分类号： C07D401/14 , A61K31/41 , C07D403/14 , C07D413/14 , A61P35/00 , A61P19/00 , C07D407/14 , C07D409/14
摘要： The disclosure generally relates to substituted heterocyclic compounds of Formula (Ia), which are inhibitors of PAD4, method for preparing these compounds, pharmaceutical compositions comprising these compounds and use of these compounds in the treatment of a disease or a disorder associated with PAD4 enzyme activity.

3. 发明申请

WO2021011724A1 TRICYCLIC HETEROARYL COMPOUNDS USEFUL AS IRAK4 INHIBITORS 审中-公开
公开(公告)号：WO2021011724A1
公开(公告)日：2021-01-21
申请号：PCT/US2020/042241
申请日：2020-07-16
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： NAIR, Satheesh Kesavan , PAIDI, Venkatram Reddy , SARKUNAM, Kandhasamy , SISTLA, Ramesh Kumar , HYNES, John , MURUGESAN, Natesan
IPC分类号： C07D471/04 , C07D471/14 , C07D498/04 , C07D491/048 , A61P35/00 , A61P29/00 , A61P37/00 , A61K31/4375
摘要： Disclosed are compounds of Formula (I) or a salt or prodrug thereof, wherein: X 1 and X 2 are independently C or N, provided that zero or one of X 1 and X 2 is N; Ring A represented by the structure is: or; and Q, R 1 , R 2 , R 3 , R 4 , R 6 , and p are define herein. Also disclosed are methods of using such compounds as modulators of IRAK4, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing inflammatory and autoimmune diseases, or in the treatment of cancer.

4. 发明申请

WO2014074675A1 HETEROARYL SUBSTITUTED PYRIDYL COMPOUNDS USEFUL AS KINASE MODULATORS 审中-公开
标题翻译：异氟醚取代的吡啶化合物可用作激酶调节剂
公开(公告)号：WO2014074675A1
公开(公告)日：2014-05-15
申请号：PCT/US2013/068875
申请日：2013-11-07
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： BHIDE, Rajeev S. , DUNCIA, John V. , HYNES, John , NAIR, Satheesh K. , PITTS, William J. , KUMAR, Sreekantha R. , GARDNER, Daniel S. , MURUGESAN, Natesan , PAIDI, Venkatram Reddy , SANTELLA, Joseph B. , SISTLA, Ramesh , WU, Hong
IPC分类号： C07D401/14 , C07D401/12 , C07D407/14 , C07D417/14 , A61K31/435
CPC分类号： C07D407/14 , C07D213/74 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D417/14
摘要： Compounds having the following formula (I) or a stereoisomer or a pharmaceutically-acceptable salt thereof, wherein R 2 is a monocyclic heteroaryl group, and R 1 , R 3 , R 4 , R 5 and R 6 are as defined herein, are useful as kinase modulators, including IRAK-4 inhibition.
摘要翻译：具有下式（I）的化合物或其立体异构体或其药学上可接受的盐，其中R 2是单环杂芳基，且R 1，R 3，R 4，R 5和R 6如本文所定义，可用作激酶调节剂，包括IRAK -4抑制。

5. 发明申请

WO2013106641A1 THIAZOLYL- OR THIADIAZOLYL-SUBSTITUTED PYRIDYL COMPOUNDS USEFUL AS KINASE INHIBITORS 审中-公开
标题翻译：作为激酶抑制剂有用的三唑基或噻二唑基取代的吡啶化合物
公开(公告)号：WO2013106641A1
公开(公告)日：2013-07-18
申请号：PCT/US2013/021134
申请日：2013-01-11
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： PAIDI, Venkatram Reddy , KUMAR, Sreekantha Ratna , NAIR, Satheesh Kesavan , BANERJEE, Abhisek , SISTLA, Ramesh , PITTS, William J. , HYNES, John
IPC分类号： C07D417/04 , C07D417/14 , A61K31/4439 , A31P37/00 , A61P29/00
CPC分类号： C07D417/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D471/04 , C07D487/04
摘要： Compounds having the following formula (I) or an enantiomer, diastereomer or a pharmaceutically-acceptable salt thereof, wherein X is N or C-R 7 , are useful as kinase modulators, including IRAK-4 modulation.
摘要翻译：具有下式（I）的化合物或其对映体，非对映异构体或其药学上可接受的盐，其中X为N或C-R7，可用作激酶调节剂，包括IRAK-4调节。

6. 发明申请

WO2016210037A1 HETEROARYL SUBSTITUTED AMINOPYRIDINE COMPOUNDS 审中-公开
标题翻译：异构取代的氨基吡啶化合物
公开(公告)号：WO2016210037A1
公开(公告)日：2016-12-29
申请号：PCT/US2016/038862
申请日：2016-06-23
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： DUNCIA, John V. , GARDNER, Daniel S. , HYNES, John , MACOR, John E. , SANTELLA, Joseph B. , WU, Hong , NAIR, Satheesh Kesavan , PAIDI, Venkatram Reddy , SARKUNAM, Kandhasamy , SISTLA, Ramesh Kumar , POLIMERA, Subba Rao
IPC分类号： C07D487/04 , A61K31/5025 , A61K31/519 , A61P37/00
CPC分类号： C07D487/04
摘要： Disclosed are compounds of Formula (I) or salts thereof, wherein: HET is a heteroaryl selected from imidazo[1,2-b]pyridazinyl and pyrazolo[1,5-a]pyrimidinyl, wherein said heteroaryl is attached to the pyridinyl group in the compound of Formula (I) by a carbon ring atom in the heteroaryl and wherein said heteroaryl is substituted with zero to 2 Rb; A is pyrazolyl, imidazolyl, or triazolyl, each substituted with zero or 1 Ra; and R3, Ra, and Rb are define herein. Also disclosed are methods of using such compounds as modulators of IRAK4, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing inflammatory and autoimmune diseases, or in the treatment of cancer.
摘要翻译：公开了式（I）的化合物或其盐，其中：HET是选自咪唑并[1,2-b]哒嗪基和吡唑并[1,5-a]嘧啶基的杂芳基，其中所述杂芳基连接到吡啶基式（I）的化合物，其中杂芳基中的碳环原子，其中所述杂芳基被0-2Rb取代; A是吡唑基，咪唑基或三唑基，各自被0或1个Ra取代; 并且R 3，R a和R b在本文中定义。还公开了使用这样的化合物作为IRAK4的调节剂的方法和包含这些化合物的药物组合物。这些化合物可用于治疗，预防或减缓炎症和自身免疫疾病或治疗癌症。

7. 发明申请

WO2016210036A1 HETEROARYL SUBSTITUTED AMINOPYRIDINE COMPOUNDS 审中-公开
标题翻译：异构取代的氨基吡啶化合物
公开(公告)号：WO2016210036A1
公开(公告)日：2016-12-29
申请号：PCT/US2016/038861
申请日：2016-06-23
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： DUNCIA, John V. , GARDNER, Daniel S. , HYNES, John , MACOR, John E. , MURUGESAN, Natessan , SANTELLA, Joseph B. , WU, Hong , KANTHETI, Durgarao , NAIR, Satheesh Kesavan , PAIDI, Venkatram Reddy , RATNA KUMAR, Sreekantha , SARKUNAM, Kandhasamy , SISTLA, Ramesh Kumar , POLIMERA, Subba Rao
IPC分类号： C07D401/14 , C07D413/04 , C07D487/04 , A61K31/435 , A61P35/00
CPC分类号： C07D487/04 , C07D401/14 , C07D413/04
摘要： Disclosed are compounds of Formula (I) Formula(I) or salts thereof, wherein HET is a heteroaryl selected from oxazolyl, pyrazolyl, imidazo[l,2-b]pyridazin-3-yl, and pyrazolo[l,5-a]pyrimidin-3-yl, wherein said heteroaryl is attached to the pyridinyl group in the compound of Formula (I) by a carbon ring atom in the heteroaryl and wherein said heteroaryl is substituted with zero to 2 R b ; and R 1 , R 3 , and R b are define herein. Also disclosed are methods of using such compounds as modulators of IRAK4, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing inflammatory and autoimmune diseases, or in the treatment of cancer.
摘要翻译：公开了式（I）式（I）的化合物或其盐，其中HET是选自恶唑基，吡唑基，咪唑并[1,2-b]哒嗪-3-基和吡唑并[1,5-a] 嘧啶-3-基，其中所述杂芳基通过杂芳基中的碳环原子与式（I）化合物中的吡啶基连接，并且其中所述杂芳基被0-2Rb取代; 并且R1，R3和Rb在本文中定义。还公开了使用这样的化合物作为IRAK4的调节剂的方法和包含这些化合物的药物组合物。这些化合物可用于治疗，预防或减缓炎症和自身免疫疾病或治疗癌症。

8. 发明申请

WO2016210034A1 HETEROARYL SUBSTITUTED AMINOPYRIDINE COMPOUNDS 审中-公开
标题翻译：异氟醚取代的氨基吡啶化合物
公开(公告)号：WO2016210034A1
公开(公告)日：2016-12-29
申请号：PCT/US2016/038858
申请日：2016-06-23
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： GARDNER, Daniel S. , SANTELLA, Joseph B. , PAIDI, Venkatram Reddy , WU, Hong , DUNCIA, John V. , NAIR, Satheesh Kesavan , HYNES, John
IPC分类号： C07D471/04 , C07D487/04 , A61K31/437 , A61K31/519 , A61P29/00
CPC分类号： C07D487/04 , C07D471/04
摘要： Disclosed are compounds of Formula (I) or salts thereof, wherein HET is a heteroaryl selected from pyrrolo[2,3 b]pyridinyl, pyrrolo[2,3 d]pyrimidinyl, pyrazolo[3,4 b]pyridinyl, pyrazolo[3,4 d]pyrimidinyl, imidazolo[4,5 b]pyridinyl, and imidazolo[4,5 d]pyrimidinyl, wherein said heteroaryl is attached to the pyridinyl group in the compound of Formula (I) by a nitrogen ring atom in said heteroaryl and wherein said heteroaryl is substituted with zero to 2 R b ; A is pyrazolyl, imidazolyl, triazolyl, isoxazolyl, oxadiazolyl or dihydroisoxazolyl, each substituted with zero or 1 R a ; and R 3 , R a , and R b are define herein. Also disclosed are methods of using such compounds as modulators of IRAK4, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing inflammatory and autoimmune diseases, or in the treatment of cancer.
摘要翻译：公开了式（I）的化合物或其盐，其中HET是选自吡咯并[2,3-b]吡啶基，吡咯并[2,3-d]嘧啶基，吡唑并[3,4-b]吡啶基，吡唑并[ 4 d]嘧啶基，咪唑并[4,5-b]吡啶基和咪唑并[4,5-d]嘧啶基，其中所述杂芳基通过所述杂芳基中的氮环原子与式（I）化合物中的吡啶基连接，其中所述杂芳基被0-2Rb取代; A是吡唑基，咪唑基，三唑基，异恶唑基，恶二唑基或二氢异恶唑基，各自被0或1个Ra取代; 并且R 3，R a和R b在本文中定义。还公开了使用这样的化合物作为IRAK4的调节剂的方法和包含这些化合物的药物组合物。这些化合物可用于治疗，预防或减缓炎症和自身免疫疾病或治疗癌症。

9. 发明申请

WO2015103453A1 HETEROARYL SUBSTITUTED NICOTINAMIDE COMPOUNDS 审中-公开
标题翻译： HETEROARYL取代的NICOTINAMIDE化合物
公开(公告)号：WO2015103453A1
公开(公告)日：2015-07-09
申请号：PCT/US2015/010006
申请日：2015-01-02
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： SANTELLA, Joseph B. , KUMAR, Sreekantha Ratna , DUNCIA, John V. , GARDNER, Daniel S. , PAIDI, Venkatram Reddy , NAIR, Satheesh Kesavan , HYNES, John , WU, Hong , MURUGESAN, Natesan , SARKUNAM, Kandhasamy , ARUNACHALAM, Piramanayagam
IPC分类号： C07D401/14 , C07D401/04 , C07D471/04 , C07D487/04 , C07D473/00 , A61P37/00 , A61P29/00 , A61K31/455 , A61K31/437 , A61K31/519 , A61K31/52
CPC分类号： C07D471/04 , C07D401/04 , C07D401/14 , C07D487/04 , C07D519/00 , C07F9/65616
摘要： Disclosed are compounds of Formula (I) or salts thereof, wherein: HET is a heteroaryl selected from pyrazolyl, indolyl, pyrrolo[2,3-b]pyridinyl, pyrrolo[2,3-d]pyrimidinyl, pyrazolo[3,4-b]pyridinyl, pyrazolo[3,4-d]pyrimidinyl, 2,3-dihydro-1H-pyrrolo[2,3-b]pyridinyl, imidazo[4,5-b] pyridinyl, and purinyl, wherein said heteroaryl is substituted with R a and R b ; and R 1 and R 2 are define herein. Also disclosed are methods of using such compounds as modulators of IRAK4, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing inflammatory and autoimmune diseases.
摘要翻译：公开了式（I）的化合物或其盐，其中：HET是选自吡唑基，吲哚基，吡咯并[2,3-b]吡啶基，吡咯并[2,3-d]嘧啶基，吡唑并[3,4- b]吡啶基，吡唑并[3,4-d]嘧啶基，2,3-二氢-1H-吡咯并[2,3-b]吡啶基，咪唑并[4,5-b]吡啶基和嘌呤基，其中所述杂芳基被取代与Ra和Rb; 并且R1和R2在本文中定义。还公开了使用这样的化合物作为IRAK4的调节剂的方法和包含这些化合物的药物组合物。这些化合物可用于治疗，预防或减缓炎症和自身免疫性疾病。

10. 发明申请

WO2013106612A1 HETEROCYCLIC-SUBSTITUTED PYRIDYL COMPOUNDS USEFUL AS KINASE INHIBITORS 审中-公开
标题翻译：杂环取代的吡啶化合物作为激酶抑制剂有用
公开(公告)号：WO2013106612A1
公开(公告)日：2013-07-18
申请号：PCT/US2013/021093
申请日：2013-01-11
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： PAIDI, Venkatram Reddy , KUMAR, Sreekantha Ratna , BANERJEE, Abhisek , NAIR, Satheesh Kesavan , SISTLA, Ramesh K. , PITTS, William J. , HYNES, John
IPC分类号： C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14 , C07D471/04 , C07D471/10 , C07D487/04 , A61P29/00 , A61K31/4427 , A61K31/443 , A61K31/4439 , A61K31/498 , A61K31/4709 , A61K31/517 , A61K31/5025
CPC分类号： C07D417/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D471/04 , C07D471/10 , C07D487/04
摘要： Compounds having the following formula: wherein A is, or; and X is N or C-R 7 , or an enantiomer, diastereomer or a pharmaceutically-acceptable salt thereof, are useful as kinase modulators, including IRAK-4 modulation.
摘要翻译：具有下式的化合物：其中A是或; 并且X是N或C-R7，或其对映体，非对映体或其药学上可接受的盐，可用作激酶调节剂，包括IRAK-4调节。

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