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1. 发明申请

WO2009030952A2 HETEROCYCLIC COMPOUNDS AND METHODS OF USE THEREOF-975 审中-公开
标题翻译：杂环化合物及其使用方法-975
公开(公告)号：WO2009030952A2
公开(公告)日：2009-03-12
申请号：PCT/GB2008/050782
申请日：2008-09-04
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , FAUBER, Benjamin , HIRD, Alexander , JANETKA, James , RUSSELL, Daniel, John , YANG, Bin
发明人： FAUBER, Benjamin , HIRD, Alexander , JANETKA, James , RUSSELL, Daniel, John , YANG, Bin
IPC分类号： C07D233/64 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/14 , C07D417/12 , C07D471/04 , A61K31/4427 , A61P35/00
CPC分类号： C07D401/12 , C07D233/64 , C07D401/14 , C07D405/12 , C07D409/14 , C07D417/12 , C07D471/04
摘要： The present disclosure relates to heterocyclic amide compounds, which are useful for inhibiting the Hedgehog pathway, and their use in treating a disease or medical condition mediated alone or in part by Hedgehog pathway inhibition. Also disclosed are methods for manufacture of these compounds, pharmaceutical compositions including these compounds, and use of these compounds in the manufacture of medicaments for treating such diseases and medical conditions in a subject.
摘要翻译：本公开涉及可用于抑制Hedgehog途径的杂环酰胺化合物及其用于治疗单独或部分由Hedgehog通路抑制介导的疾病或医学病症的用途。还公开了制备这些化合物的方法，包括这些化合物的药物组合物，以及这些化合物在制备用于治疗受试者的这些疾病和医疗状况的药物中的用途。

2. 发明申请

WO2009027746A1 HETEROCYCLIC AMIDES USEFUL FOR THE TREATMENT OF CANCER AND PSORIASIS 审中-公开
标题翻译：用于治疗癌症和PSORIASIS的杂环类药物有用
公开(公告)号：WO2009027746A1
公开(公告)日：2009-03-05
申请号：PCT/GB2008/050756
申请日：2008-08-29
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , DAKIN, Leslie , FAUBER, Benjamin , HIRD, Alexander , JANETKA, James , RUSSELL, Daniel, John , SU, Qibin , YANG, Bin , ZHENG, XiaoLan
发明人： DAKIN, Leslie , FAUBER, Benjamin , HIRD, Alexander , JANETKA, James , RUSSELL, Daniel, John , SU, Qibin , YANG, Bin , ZHENG, XiaoLan
IPC分类号： C07D213/30 , C07D213/40 , C07D213/73 , C07D233/61 , C07D401/12 , C07D413/12 , C07D417/12 , C07D417/14 , C07D473/00 , C07D513/04 , A61K31/40 , A61K31/41 , A61K31/435 , A61K31/4427 , A61P35/00
CPC分类号： C07D401/12 , C07D213/30 , C07D213/40 , C07D213/73 , C07D233/61 , C07D413/12 , C07D417/12 , C07D417/14 , C07D473/00 , C07D513/04
摘要： The present disclosure relates to heterocyclic amide compounds, which are useful for inhibiting the Hedgehog pathway, and their use in treating a disease or medical condition mediated alone or in part by Hedgehog pathway inhibition. Also disclosed are methods for manufacture of these compounds, pharmaceutical compositions including these compounds, and use of these compounds in the manufacture of medicaments for treating such diseases and medical conditions in a subject. Formula (IA) with the provisio that either R 2 or R 3 is (Z).
摘要翻译：本公开涉及可用于抑制Hedgehog途径的杂环酰胺化合物及其用于治疗单独或部分由Hedgehog通路抑制介导的疾病或医学病症的用途。还公开了制备这些化合物的方法，包括这些化合物的药物组合物，以及这些化合物在制备用于治疗受试者的这些疾病和医疗状况的药物中的用途。式（IA），条件是R 2或R 3为（Z）。

3. 发明申请

WO2006106326A1 SUBSTITUTED HETEROCYCLES AND THEIR USE AS CHK1, PDK1 AND PAK INHIBITORS 审中-公开
标题翻译：取代的杂环化合物及其用作CHK1，PDK1和PAK抑制剂
公开(公告)号：WO2006106326A1
公开(公告)日：2006-10-12
申请号：PCT/GB2006/001242
申请日：2006-04-05
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , DALY, Kevin , HERON, Nicola , HIRD, Alexander , IOANNIDIS, Stephanos , JANETKA, James, Walter , LYNE, Paul , SCOTT, Jamie , TOADER, Dorin , VASBINDER, Melissa , YU, Dingwei , YU, Yan
发明人： DALY, Kevin , HERON, Nicola , HIRD, Alexander , IOANNIDIS, Stephanos , JANETKA, James, Walter , LYNE, Paul , SCOTT, Jamie , TOADER, Dorin , VASBINDER, Melissa , YU, Dingwei , YU, Yan
IPC分类号： C07D495/04 , C07D209/12 , C07D513/04 , C07D209/14 , C07D491/04 , C07D401/04 , C07D209/08 , C07D235/18 , C07D209/10 , A61K31/4365 , A61K31/404 , A61K31/4184 , A61K31/4439 , A61K31/437 , A61K31/4355
CPC分类号： C07D491/04 , C07D401/12 , C07D401/14 , C07D495/04 , C07D513/04
摘要： This invention relates to novel compounds of Formula (I) and to their pharmaceutical compositions and to their methods of use. These novel compounds possess CHK1 kinase inhibitory activity, PDK1 inhibitory activity and Pak kinase inhibitory activity and are accordingly useful in the treatment and/or prophylaxis of cancer.
摘要翻译：本发明涉及新的式（I）化合物及其药物组合物及其使用方法。这些新化合物具有CHK1激酶抑制活性，PDK1抑制活性和Pak激酶抑制活性，因此可用于治疗和/或预防癌症。

4. 发明申请

WO2010142994A1 2, 3-DIHYDRO-1H-INDENE COMPOUNDS AND THEIR USE TO TREAT CANCER 审中-公开
标题翻译： 2，3-DIHYDRO-1H-INDENE化合物及其用于治疗癌症
公开(公告)号：WO2010142994A1
公开(公告)日：2010-12-16
申请号：PCT/GB2010/050973
申请日：2010-06-10
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , AQUILA, Brian , HENNESSY, Edward , HIRD, Alexander , OZA, Vibha , SAEH, Jamel Carlos , SHA, Li
发明人： AQUILA, Brian , HENNESSY, Edward , HIRD, Alexander , OZA, Vibha , SAEH, Jamel Carlos , SHA, Li
IPC分类号： C07D403/12 , A61K31/4025 , A61P35/00
CPC分类号： C07D403/12
摘要： Provided herein are 2,3-dihydro-1H-indene compounds, methods for making the compounds, pharmaceutical compositions containing the compounds. The described compounds inhibit IAP proteins and can be used to treat various cancers.
摘要翻译：本文提供了2,3-二氢-1H-茚化合物，制备该化合物的方法，含有这些化合物的药物组合物。所述的化合物抑制IAP蛋白并可用于治疗各种癌症。

5. 发明申请

WO2018178227A1 SYNTHESIS OF MCL-1 INHIBITOR 审中-公开
公开(公告)号：WO2018178227A1
公开(公告)日：2018-10-04
申请号：PCT/EP2018/058056
申请日：2018-03-29
申请人： ASTRAZENECA AB
发明人： STEWART, Craig , HARDY, Simon , STARK, Andrew , HIRD, Alexander , YE, Qing , ZHENG, Xiaolan , FERRAR, Cati , KOEK, Jan , HAZRA, Debasis
IPC分类号： C07D231/12 , C07D403/04 , C07C245/06
摘要： Disclosed are intermediates and methods of synthesizing Compound 1.

6. 发明申请

WO2017001354A1 POLYCYCLIC AMIDE DERIVATIVES AS CDK9 INHIBITORS 审中-公开
标题翻译：多环酰胺衍生物作为CDK9抑制剂
公开(公告)号：WO2017001354A1
公开(公告)日：2017-01-05
申请号：PCT/EP2016/064899
申请日：2016-06-27
申请人： ASTRAZENECA AB
发明人： PIKE, Kurt, Gordon , BARLAAM, Bernard, Christophe , HAWKINS, Janet , DE SAVI, Christopher , VASBINDER, Melissa, Marie , HIRD, Alexander , LAMB, Michelle
IPC分类号： C07D471/04 , C07D487/04 , C07D498/04 , A61K31/437 , A61P35/00
CPC分类号： C07D498/04 , C07B2200/13 , C07D471/04 , C07D487/04
摘要： Provided are a series of novel pyridine or pyrimidine derivatives of Formula (I) which inhibit CDK9 and may be useful for the treatment of hyperproliferative diseases. In particular the compounds are of use in the treatment of proliferative diseases such as cancer including hematological malignancies such as acute myeloid leukemia, multiple myeloma, chronic lymphocytic leukemia, diffuse large B cell lymphoma, Burkitt's lymphoma, follicular lymphoma and solid tumors such as breast cancer, lung cancer, neuroblastoma and colon cancer. A is C(R 5 ) or N; R 5 is H, C 1-3 alkyl, CN or halogen; R 2 is optionally substituted 3-7 membered heterocycloalkyl or 3-7 membered cycloalkyl; R 4 is (A) or (B) wherein X and Y together with the atoms to which they are attached form an optionally substituted, saturated or partially saturated 5 to 7 membered heterocycloalkyl ring which, in addition to the bridge nitrogen, may contain one or two heteroatoms selected from N, O, and S; J is N or CR 11 ; and R 11 is H or C 1-3 alkyl.
摘要翻译：提供一系列抑制CDK9的式（I）的吡啶或嘧啶衍生物，可用于治疗过度增殖性疾病。特别地，这些化合物可用于治疗增殖性疾病如癌症，包括血液恶性肿瘤例如急性骨髓性白血病，多发性骨髓瘤，慢性淋巴细胞白血病，弥漫性大B细胞淋巴瘤，伯基特淋巴瘤，滤泡淋巴瘤和实体瘤如乳腺癌，肺癌，成神经细胞瘤和结肠癌。 A为C（R5）或N; R5是H，C1-3烷基，CN或卤素; R2是任选取代的3-7元杂环烷基或3-7元环烷基; R4是（A）或（B）其中X和Y与它们连接的原子一起形成任选取代的，饱和或部分饱和的5至7元杂环烷基环，除了桥氮之外，其还可以含有一个或多个两个选自N，O和S的杂原子; J为N或CR11; R 11为H或C 1-3烷基。

7. 发明申请

WO2018178226A1 MCL-1 INHIBITORS AND METHODS OF USE THEREOF 审中-公开
公开(公告)号：WO2018178226A1
公开(公告)日：2018-10-04
申请号：PCT/EP2018/058054
申请日：2018-03-29
申请人： ASTRAZENECA AB
发明人： PACKER, Martin, John , PERKINS, David, Robert , SWALLOW, Steven , HIRD, Alexander , YE, Qing , PENG, Bo , ZHENG, Xiaolan , JOHANNES, Jeffrey , MLYNARSKI, Scott , LAMB, Michelle , HUYNH, Hoan , ROBBINS, Daniel, William
IPC分类号： C07D515/22 , A61P35/00 , A61K31/395
CPC分类号： C07D515/22 , A61P35/00
摘要： Disclosed are Mcl-1 inhibitors, pharmaceutical compositions comprising the same and methods of using the same.

8. 发明申请

WO2017182625A1 MACROCYCLIC MCL1 INHIBITORS FOR TREATING CANCER 审中-公开
标题翻译：用于治疗癌症的大环MCL1抑制剂
公开(公告)号：WO2017182625A1
公开(公告)日：2017-10-26
申请号：PCT/EP2017/059511
申请日：2017-04-21
申请人： ASTRAZENECA AB
发明人： HIRD, Alexander , BELMONTE, Matthew, Alan , YANG, Wenzhan , SECRIST, John, Paul , ROBBINS, Daniel, William , KAZMIRSKI, Steven, Lee , WU, Dedong , PENG, Bo , JOHANNES, Jeffrey , LAMB, Michelle, Laurae , YE, Oing , ZHENG, Xiaolan
IPC分类号： C07D515/22 , A61K31/395 , A61P35/00
摘要： Disclosed is a compound which is 17-chloro-5,13,14,22-tetramethyl-28-oxa-2,9-dithia-5,6,12,13,22-pentaazaheptacyclo[27.7.1.14,7.011,15.016,21.020,24.030,35]octatriaconta- 1(37),4(38),6,11,14,16,18,20,23,29,31,33,35-tridecaene-23-carboxylic acid (Formula I) and enantiomers and pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions of 17-chloro-5,13,14,22-tetramethyl-28-oxa-2,9-dithia- 5,6,12,13,22-pentaazaheptacyclo[27.7.1.14,7.011,15.016,21.020,24.030,35]octatriaconta- 1(37),4(38),6,11,14,16,18,20,23,29,31,33,35-tridecaene-23-carboxylic acid, and enantiomers and pharmaceutically acceptable salts thereof, and methods of treating cancer with such compounds and compositions.
摘要翻译：公开了17-氯-5,13,14,22-四甲基-28-氧杂-2,9-二硫杂-5,6,12,13,22-五氮杂环庚二烯并[4,5-b] （37），4（38），6,11,14,16,18,20,23,29,31,33,35-十三碳-7-烯，（式I）及其对映体和药学上可接受的盐。还公开了17-氯-5,13,14,22-四甲基-28-氧杂-2,9-二硫杂-5,6,12,13,22-五氮杂七环[27.7.1.14,7.011,15.016，（37），4（38），6,11,14,16,18,20,23,29,31,33,35-十三碳烯-23-羧酸，以及对映体和其药学上可接受的盐，以及用这些化合物和组合物治疗癌症的方法。

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