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1. 发明申请

WO2018005435A1 4,6-DIAMINOQUINAZOLINES AS COT MODULATORS AND METHODS OF USE THEREOF 审中-公开
标题翻译： 4,6-二氨基喹唑啉作为COT调节剂及其使用方法
公开(公告)号：WO2018005435A1
公开(公告)日：2018-01-04
申请号：PCT/US2017/039418
申请日：2017-06-27
申请人： GILEAD SCIENCES, INC.
发明人： BALAN, Gayatri , CHOU, Chien-Hung , KIM, Musong , KIRSCHBERG, Thorsten A. , LINK, John O. , PHILLIPS, Gary , SAITO, Roland D. , SQUIRES, Neil H. , TAYLOR, James G. , WATKINS, William J. , WRIGHT, Nathan E.
IPC分类号： C07D403/12 , C07D401/14 , C07D405/14 , C07D417/14 , A61K31/517 , A61P35/00 , A61P29/00 , A61P3/10
摘要： The invention relates to 4,6-diaminoquinazoline derivatives of formula I which are modulators of the Cot (cancer Osaka thyroid) kinase, also known as MAP3K8, EST or Tlp-2, and their use for treating e.g. cancer, diabetes and inflammatory diseases.
摘要翻译：本发明涉及作为Cot（癌症大阪甲状腺）激酶（也称为MAP3K8，EST或Tlp-2）的调节剂的式I的4,6-二氨基喹唑啉衍生物及其用于治疗例如癌症，糖尿病和炎症性疾病。

2. 发明申请

WO2011143106A1 BI - FUNCTIONAL PYRAZOLOPYRIDINE COMPOUNDS 审中-公开
标题翻译：双功能吡唑啉化合物
公开(公告)号：WO2011143106A1
公开(公告)日：2011-11-17
申请号：PCT/US2011/035741
申请日：2011-05-09
申请人： GILEAD SCIENCES, INC. , BAKER, William, R. , CAI, Shaopei , KAPLAN, Joshua, Aaron , KIM, Musong , PHILLIPS, Gary , PURVIS, II., Lafe, J. , STASIAK, Marcin , STEVENS, Kirk, L. , VAN VELDHUIZEN, Josh
发明人： BAKER, William, R. , CAI, Shaopei , KAPLAN, Joshua, Aaron , KIM, Musong , PHILLIPS, Gary , PURVIS, II., Lafe, J. , STASIAK, Marcin , STEVENS, Kirk, L. , VAN VELDHUIZEN, Josh
IPC分类号： C07D471/04 , A61K31/437 , A61P29/00 , A61P37/08
CPC分类号： C07D471/04
摘要： invention provides compounds of the formula: wherein R 1 and R 2 together with the phenyl to which they are bound may form a bicyclic, fused heterocyclic ring and all other variables are as defined herein, their use in pulmonary inflammation or bronchoconstriction therapy and compositions comprising and processes for preparing the same are provided.
摘要翻译：本发明提供下式的化合物：其中R 1和R 2与它们所连接的苯基一起可以形成双环稠合杂环，并且所有其它变量如本文所定义，它们在肺部炎症或支气管收缩治疗中的用途以及包含和过程提供了相同的准备。

3. 发明申请

WO2020092621A1 SUBSTITUTED 6-AZABENZIMIDAZOLE COMPOUNDS AS HPK1 INHIBITORS 审中-公开
公开(公告)号：WO2020092621A1
公开(公告)日：2020-05-07
申请号：PCT/US2019/058932
申请日：2019-10-30
申请人： GILEAD SCIENCES, INC.
发明人： BALAN, Gayatri , BARTLETT, Mark J. , CHANDRASEKHAR, Jayaraman , CODELLI, Julian A. , CONWAY, John H. , COSMAN, Jennifer L. , KALLA, Rao V. , KASUN, Zachary A. , KIM, Musong , LEE, Seung H. , LO, Jennifer R. , LOYER-DREW, Jennifer A. , MITCHELL, Scott A. , PERRY, Thao D. , PHILLIPS, Gary B. , SALVO, Patrick J. , SWAMINATHAN, Sundaramoorthi , VAN VELDHUIZEN, Joshua J. , YEUNG, Suet C. , ZABLOCKI, Jeff
IPC分类号： C07D471/04 , C07D519/00 , A61K31/437 , A61P35/00
摘要： The present disclosure relates generally to certain 6-azabenzimidazole compounds, pharmaceutical compositions comprising said compounds, and methods of making and using said compounds and pharmaceutical compositions. The compounds and compositions disclosed herein may be used for the treatment or prevention of diseases, disorders, or infections modifiable by hematopoietic progenitor kinase 1 (HPK1) inhibitors, such as HBV, HIV, cancer, and/or a hyper-proliferative disease.

4. 发明申请

WO2015191754A2 PHOSPHATIDYLINOSITOL 3-KINASE INHIBITORS 审中-公开
标题翻译：磷酸胆碱3-激酶抑制剂
公开(公告)号：WO2015191754A2
公开(公告)日：2015-12-17
申请号：PCT/US2015/035161
申请日：2015-06-10
申请人： GILEAD SCIENCES, INC.
发明人： KIM, Musong , YEUNG, Suet, Chung , PERREAULT, Stephane
IPC分类号： C07D403/14
CPC分类号： C07D403/14 , C07D471/04 , C07D487/04 , C07D491/048
摘要： The present application provides the compounds of formula (J), or pharmaceutically acceptable salts, isomers, tautomer, or a mixture thereof wherein n, m, R 1 , R 2 , R 3 , R 4 , and R 5 are described herein. The compounds are inhibitors to the activities of phosphatidylinositol 3-kinase (ΡI3Κ) and are useful for treating conditions mediated by one or more PI3K isoforms. The present application further provides pharmaceutical compositions that include a compound of formula (I), or pharmaceutically acceptable salts, isomers, tautomer, or mixture thereof, and methods of using these compounds and compositions for treating conditions mediated by one or more ΡI3Κ isoforms.
摘要翻译：本申请提供式（J）化合物或其药学上可接受的盐，异构体，互变异构体或其混合物，其中n，m，R 1，R 2，R 3，R 4和R 5在本文中描述。这些化合物是磷脂酰肌醇3-激酶（ΡI3K）活性的抑制剂，可用于治疗由一种或多种PI3K同种型介导的病症。本申请还提供包含式（I）化合物或其药学上可接受的盐，异构体，互变异构体或其混合物的药物组合物，以及使用这些化合物和组合物治疗由一种或多种PIP3κ同种型介导的病症的方法。

5. 发明申请

WO2010126953A1 CORTICOSTEROID LINKED BETA-AGONIST COMPOUNDS FOR USE IN THERAPY 审中-公开
标题翻译：用于治疗的角质层连接的抗原激动剂化合物
公开(公告)号：WO2010126953A1
公开(公告)日：2010-11-04
申请号：PCT/US2010/032689
申请日：2010-04-28
申请人： GILEAD SCIENCES, INC. , BAKER, William, R. , KIM, Musong , PHILLIPS, Gary , RUDOLPH, Alexander , STASIAK, Marcin
发明人： BAKER, William, R. , KIM, Musong , PHILLIPS, Gary , RUDOLPH, Alexander , STASIAK, Marcin
IPC分类号： C07J41/00 , C07J43/00 , C07J71/00 , A61K31/573 , A61K31/58 , A61P5/44
CPC分类号： C07J41/005 , C07J43/003 , C07J71/0031
摘要： New chemical entities which comprise corticosteroids and phosphorylated β- agonists for use in therapy and compositions comprising and processes for preparing the same are provided.
摘要翻译：提供了包含用于治疗的皮质类固醇和磷酸化β-激动剂的新化学实体及其制备方法及其制备方法。

6. 发明申请

WO2015200352A1 PHOSPHATIDYLINOSITOL 3-KINASE INHIBITORS 审中-公开
标题翻译：磷酸胆碱3-激酶抑制剂
公开(公告)号：WO2015200352A1
公开(公告)日：2015-12-30
申请号：PCT/US2015/037234
申请日：2015-06-23
申请人： GILEAD SCIENCES, INC.
发明人： EVARTS, Jerry , KAPLAN, Joshua , KIM, Musong , NADUTHAMBI, Devan , PATEL, Leena , PERRAULT, Stephane , PHILLIPS, Gary , PURVIS, Lafe, J., II , STEVENS, Kirk, L. , TREIBERG, Jennifer, A.
IPC分类号： C07D403/12 , C07D401/14 , C07D413/14 , C07D403/14 , C07D409/14 , C07D491/107 , A61K31/517 , A61P35/00 , A61P37/00 , A61P29/00
CPC分类号： C07D403/12 , C07D401/14 , C07D403/14 , C07D409/14 , C07D413/14 , C07D491/107
摘要： The present disclosure provides phosphatidylinositol 3-kinase (PI3K) inhibitors of formula (J), or pharmaceutically acceptable salts thereof, in which A, n, m, R 1 , R 2 , R 3 R 4 , R 5 , R 6 and R 7 are as defined herein. These compounds are useful for treatment of conditions mediated by one or more ΡI3Κ isoforms. The present disclosure further provides pharmaceutical compositions that include a compound of formula (J), or pharmaceutically acceptable salts thereof, and methods of using these compounds and compositions to treat conditions mediated by one or more PI3K isoforms.
摘要翻译：本公开提供式（J）的磷脂酰肌醇3-激酶（PI3K）抑制剂或其药学上可接受的盐，其中A，n，m，R 1，R 2，R 3，R 4，R 6，R 7和R 7如本文所定义。这些化合物可用于治疗由一种或多种P 1 K 3同种型介导的病症。本公开进一步提供了包含式（J）化合物或其药学上可接受的盐的药物组合物，以及使用这些化合物和组合物来治疗由一种或多种PI3K同种型介导的病症的方法。

7. 发明申请

WO2015191726A1 PHOSPHATIDYLINOSITOL 3-KINASE INHIBITORS 审中-公开
标题翻译：磷酸胆碱3-激酶抑制剂
公开(公告)号：WO2015191726A1
公开(公告)日：2015-12-17
申请号：PCT/US2015/035126
申请日：2015-06-10
申请人： GILEAD SCIENCES, INC.
发明人： CAI, Shaopei , DU, Zhimin , KIM, Musong , LOYER-DREW, Jennifer, A. , NADUTHAMBI, Devan , PATEL, Leena , PHILLIPS, Barton, W. , PHILLIPS, Gary , STEVENS, Kirk, L. , TREIBERG, Jennifer, Anne , VAN VELDHUIZEN, Joshua , WATKINS, William, J. , YEUNG, Suet, Chung
IPC分类号： C07D403/12 , C07D401/14 , C07D403/14 , C07D473/34 , C07D487/04 , C07D513/04 , A61K31/517 , A61P35/00 , A61P37/00 , A61P25/28 , A61P3/08 , A61P9/10
CPC分类号： C07D403/12 , C07D401/14 , C07D403/14 , C07D405/14 , C07D413/14 , C07D471/04 , C07D473/34 , C07D487/04 , C07D513/04
摘要： The present application provides the compounds of formula (J), or pharmaceutically acceptable salts, isomers, tautomer, or a mixture thereof, wherein n, W, A', B', R 1 , R 2 , and R 3 are described herein. The compounds are inhibitors to the activities of phosphatidylinositol 3-kinase (PI3K) and are useful for treating conditions mediated by one or more PI3K isoforms. The present application further provides pharmaceutical compositions that include a compound of formula (I), or pharmaceutically acceptable salts, isomers, tautomer, or mixture thereof, and methods of using these compounds and compositions for treating conditions mediated by one or more PI3K isoforms.
摘要翻译：本申请提供式（J）化合物或其药学上可接受的盐，异构体，互变异构体或其混合物，其中本文描述了n，W，A'，B'，R 1，R 2和R 3。这些化合物是磷脂酰肌醇3-激酶（PI3K）活性的抑制剂，可用于治疗由一种或多种PI3K同种型介导的病症。本申请还提供包含式（I）化合物或其药学上可接受的盐，异构体，互变异构体或其混合物的药物组合物，以及使用这些化合物和组合物治疗由一种或多种PI3K同种型介导的病症的方法。

8. 发明申请

WO2014201409A1 PHOSPHATIDYLINOSITOL 3-KINASE INHIBITORS 审中-公开
标题翻译：磷酸胆碱3-激酶抑制剂
公开(公告)号：WO2014201409A1
公开(公告)日：2014-12-18
申请号：PCT/US2014/042392
申请日：2014-06-13
申请人： GILEAD SCIENCES, INC.
发明人： EVARTS, Jerry , KAPLAN, Joshua , KIM, Musong , PATEL, Leena , PERREAULT, Stephane , PHILLIPS, Gary , TREIBERG, Jennifer, A. , VAN VELDHUIZEN, Joshua
IPC分类号： C07D401/14 , A61K31/47 , A61P35/00
CPC分类号： C07D401/14 , A61K31/517
摘要： The present disclosure provides phosphatidylinositol 3 -kinase (PI3K) inhibitors of formula (I), or pharmaceutically acceptable salts or isomers thereof, in which n, m, R 1 , R 2 , R 4 , and R 3 are as defined herein. These compounds are useful for treatment of conditions mediated by one or more PI3K isoforms, such as PI3Kδ. The present disclosure further provides pharmaceutical compositions that include a compound of formula (I), or pharmaceutically acceptable salts or isomers thereof, and methods of using these compounds and compositions to treat conditions mediated by one or more PI3K isoforms, such as PI3Kδ.
摘要翻译：本公开提供式（I）的磷脂酰肌醇3-激酶（PI3K）抑制剂或其药学上可接受的盐或异构体，其中n，m，R 1，R 2，R 4和R 3如本文所定义。这些化合物可用于治疗由一种或多种PI3K异构体如PI3Kδ介导的病症。本公开进一步提供了包含式（I）化合物或其药学上可接受的盐或异构体的药物组合物，以及使用这些化合物和组合物治疗由一种或多种PI3K异构体如PI3Kδ介导的病症的方法。

9. 发明申请

WO2015191745A1 PHOSPHATIDYLINOSITOL 3-KINASE INHIBITORS 审中-公开
标题翻译：磷酸胆碱3-激酶抑制剂
公开(公告)号：WO2015191745A1
公开(公告)日：2015-12-17
申请号：PCT/US2015/035147
申请日：2015-06-10
申请人： GILEAD SCIENCES, INC.
发明人： DU, Zhimin , EVARTS, Jerry , KAPLAN, Joshua , KIM, Musong , NADUTHAMBI, Devan , PATEL, Leena , PERREAULT, Stephane , PHILLIPS, Barton, W. , PHILLIPS, Gary , STEVENS, Kirk, L. , TREIBERG, Jennifer , VAN VELDHUIZEN, Joshua , WATKINS, William, J. , YEUNG, Suet, Chung
IPC分类号： C07D471/04 , C07D403/12 , C07D413/14 , C07D403/14 , C07D239/91 , C07D487/04 , C07D513/04 , A61P35/00 , A61P25/00 , A61K31/517
CPC分类号： C07D513/04 , C07D239/91 , C07D401/14 , C07D403/12 , C07D403/14 , C07D413/14 , C07D473/34 , C07D487/04
摘要： The present application provides the compounds of formula (J), or pharmaceutically acceptable salts, isomers, or a mixture thereof, wherein n, m, q, A', W 1 , W 2 , W 3 , R 1 , R 2 , and R 3 are described herein. The compounds are inhibitors to the activities of phosphatidylinositol 3-kinase (PI3K) and are useful for treating conditions mediated by one or more PI3K isoforms. The present application further provides pharmaceutical compositions that include a compound of formula (J), or pharmaceutically acceptable salts, isomers, tautomer, or mixture thereof, and methods of using these compounds and compositions for treating conditions mediated by one or more PI3K isoforms.
摘要翻译：本申请提供式（J）化合物或其药学上可接受的盐，异构体或其混合物，其中n，m，q，A'，W 1，W 2，W 3，R 1，R 2和R 3在本文中描述。这些化合物是磷脂酰肌醇3-激酶（PI3K）活性的抑制剂，可用于治疗由一种或多种PI3K同种型介导的病症。本申请还提供包含式（J）化合物或其药学上可接受的盐，异构体，互变异构体或其混合物的药物组合物，以及使用这些化合物和组合物治疗由一种或多种PI3K同种型介导的病症的方法。

10. 发明申请

WO2011081937A1 CORTICOSTEROID-BETA-AGONIST-MUSCARINIC ANTAGONIST COMPOUNDS FOR USE IN THERAPY 审中-公开
标题翻译：用于治疗的角质甾体 - 激动剂 - 肌酸拮抗剂化合物
公开(公告)号：WO2011081937A1
公开(公告)日：2011-07-07
申请号：PCT/US2010/060312
申请日：2010-12-14
申请人： GILEAD SCIENCES, INC. , BAKER, William, R. , KIM, Musong , PHILLIPS, Gary
发明人： BAKER, William, R. , KIM, Musong , PHILLIPS, Gary
IPC分类号： C07J51/00 , A61K31/573 , A61P11/06 , A61P11/08 , A61P5/44
CPC分类号： C07J51/00
摘要： The instant invention relates to new chemical entities which comprise corticosteroids, phosphorylated β-agonists and muscarinic (M3) antagonists for use in therapy and compositions comprising and processes for preparing the same.
摘要翻译：本发明涉及包含用于治疗的皮质类固醇，磷酸化β-激动剂和毒蕈碱（M3）拮抗剂的新化学物质，以及包含其制备方法的组合物。

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