公开(公告)号：US20240246937A1

公开(公告)日：2024-07-25

申请号：US18556196

申请日：2022-04-28

Applicant: George Madalin GIAMBASU ,  Andrew M. HAIDLE ,  Brett A. HOPKINS ,  James P. JEWELL ,  Matthew A. LARSEN ,  Charles A. LESBURG ,  Ping LIU ,  Qinglin PU ,  Sulagna SANYAL ,  Phieng SILIPHAIVANH ,  Matthew TUDOR ,  Catherine M. WHITE ,  Xin YAN ,  Lianyun ZHAO ,  Xiao Mei ZHENG ,  William P. KAPLAN ,  Michaelyn Claire LUX ,  Derun LI ,  Rebecca JOHNSON ,  MERCK SHARP & DOHME LLC ,  MSD R&D (CHINA) CO., LTD.

Inventor： George Madalin GIAMBASU ,  Andrew M. HAIDLE ,  Brett A. HOPKINS ,  James P. JEWELL ,  Matthew A. LARSEN ,  Charles A. LESBURG ,  Ping LIU ,  Qinglin PU ,  Sulagna SANYAL ,  Phieng SILIPHAIVANH ,  Matthew TUDOR ,  Catherine M. WHITE ,  Xin YAN ,  Lianyun ZHAO ,  Xiao Mei ZHENG ,  William P. KAPLAN ,  Michaelyn Claire LUX ,  Derun LI ,  Rebecca JOHNSON

IPC: C07D403/06 ,  C07D401/06 ,  C07D401/14 ,  C07D403/10 ,  C07D413/06 ,  C07D413/14 ,  C07D417/06 ,  C07D417/14 ,  C07D487/04

CPC classification number: C07D403/06 ,  C07D401/06 ,  C07D401/14 ,  C07D403/10 ,  C07D413/06 ,  C07D413/14 ,  C07D417/06 ,  C07D417/14 ,  C07D487/04

Abstract: The invention discloses a synthesizing method of benzimidazole derivant and intermediate, which is characterized by the following: proceeding arylation among aryl halide and primary amine; adopting L-pro as additive, cuprous iodide as catalyst; proceeding molecular arylation coupling reaction for aryl iodide or aryl bromide and primary amine; adopting iodo phenylamine compound and bromophenylamine compound as starting material; synthesizing the material through several-step transformation.

公开(公告)号：US09227971B2

公开(公告)日：2016-01-05

申请号：US13520274

申请日：2011-01-18

Applicant: M. Arshad Siddiqui ,  Yang Nan ,  Mehul F. Patel ,  Panduranga Adulla P. Reddy ,  Umar Faruk Mansoor ,  Zhaoyang Meng ,  Lalanthi Dilrukshi Vitharana ,  Lianyun Zhao ,  Amit K. Mandal ,  Duan Liu ,  Shuyi Tang ,  Andrew McRiner ,  David B. Belanger ,  Patrick J. Curran ,  Chaoyang Dai ,  Angie R. Angeles ,  Liping Yang ,  Matthew Hersh Daniels

Inventor： M. Arshad Siddiqui ,  Yang Nan ,  Mehul F. Patel ,  Panduranga Adulla P. Reddy ,  Umar Faruk Mansoor ,  Zhaoyang Meng ,  Lalanthi Dilrukshi Vitharana ,  Lianyun Zhao ,  Amit K. Mandal ,  Duan Liu ,  Shuyi Tang ,  Andrew McRiner ,  David B. Belanger ,  Patrick J. Curran ,  Chaoyang Dai ,  Angie R. Angeles ,  Liping Yang ,  Matthew Hersh Daniels

IPC: C07D487/04 ,  A61K31/519 ,  C07D471/08 ,  C07D498/08 ,  C07D491/147 ,  C07D487/08 ,  C07D513/08 ,  C07D519/00 ,  A61P35/00

CPC classification number: C07D471/08 ,  C07D487/04 ,  C07D487/08 ,  C07D491/147 ,  C07D498/08 ,  C07D513/08 ,  C07D519/00

Abstract: The present invention provides Pyrazolopyrimidine Compounds of Formula (I): wherein L, T, Z, U, V, W, R3, R6, R7, R8, and m are as defined herein, and pharmaceutically acceptable salts of such Pyrazolopyrimidine Compounds. The Pyrazolopyrimidine Compounds are useful in the treatment of cancer and other diseases or disorders wherein mTOR is deregulated.

Abstract translation: 本发明提供式（I）的吡唑并嘧啶化合物：其中L，T，Z，U，V，W，R 3，R 6，R 7，R 8和m如本文所定义，以及这些吡唑并嘧啶化合物的药学上可接受的盐。 吡唑并嘧啶化合物可用于治疗其中mTOR失调的癌症和其它疾病或病症。

公开(公告)号：US20130150362A1

公开(公告)日：2013-06-13

申请号：US13818177

申请日：2011-08-22

Applicant: Lianyun Zhao ,  Duan Liu ,  Shuyi Tang ,  Amit K. Mandal ,  Umar Faruk Mansoor ,  Lalanthi Dilrukshi Vitharana ,  Panduranga Adulla P. Reddy ,  M. Arshad Siddiqui

Inventor： Lianyun Zhao ,  Duan Liu ,  Shuyi Tang ,  Amit K. Mandal ,  Umar Faruk Mansoor ,  Lalanthi Dilrukshi Vitharana ,  Panduranga Adulla P. Reddy ,  M. Arshad Siddiqui

IPC: C07D487/04 ,  A61K31/519 ,  A61K31/5377 ,  A61K45/06

CPC classification number: C07D487/04 ,  A61K31/519 ,  A61K31/5377 ,  A61K45/06

Abstract: The present invention relates to certain pyrazolo[1,5-a]pyrimidine compounds of Formula (I) as inhibitors of mammalian Target Of Rapamycin (mTOR) kinase, which is also known as FRAP, RAFT, RAPT or SEP. The compounds may be used in the treatment of cancer and other disorders where mTOR is deregulated. The present invention further provides pharmaceutical compositions comprising the pyrazolo[1,5-a]pyrimidine compounds.

Abstract translation: 本发明涉及作为哺乳动物雷帕霉素靶标（mTOR）激酶的抑制剂的式（I）的吡唑并[1,5-a]嘧啶化合物，其也称为FRAP，RAFT，RAPT或SEP。 所述化合物可用于治疗其中mTOR失调的癌症和其它病症。 本发明还提供包含吡唑并[1,5-a]嘧啶化合物的药物组合物。

公开(公告)号：US20120322791A1

公开(公告)日：2012-12-20

申请号：US13520274

申请日：2011-01-18

Applicant: M. Arshad Siddiqui ,  Yang Nan ,  Mehul F. Patel ,  Panduranga Adulla P. Reddy ,  Umar Faruk Mansoor ,  Zhaoyang Meng ,  Lalanthi Dilrukshi Vitharana ,  Lianyun Zhao ,  Amit K. Mandal ,  Duan Liu ,  Shuyi Tang ,  Andrew McRiner ,  David B. Belanger ,  Patrick J. Curran ,  Chaoyang Dai ,  Angie R. Angeles ,  Liping Yang ,  Matthew Hersh Daniels

Inventor： M. Arshad Siddiqui ,  Yang Nan ,  Mehul F. Patel ,  Panduranga Adulla P. Reddy ,  Umar Faruk Mansoor ,  Zhaoyang Meng ,  Lalanthi Dilrukshi Vitharana ,  Lianyun Zhao ,  Amit K. Mandal ,  Duan Liu ,  Shuyi Tang ,  Andrew McRiner ,  David B. Belanger ,  Patrick J. Curran ,  Chaoyang Dai ,  Angie R. Angeles ,  Liping Yang ,  Matthew Hersh Daniels

IPC: A61K31/519 ,  A61K31/5377 ,  C07D487/08 ,  A61K31/55 ,  A61P35/00 ,  C07D498/08 ,  A61K31/5386 ,  C07D513/08 ,  A61K31/547 ,  C07D491/147 ,  C07D487/04 ,  C07D471/08

CPC classification number: C07D471/08 ,  C07D487/04 ,  C07D487/08 ,  C07D491/147 ,  C07D498/08 ,  C07D513/08 ,  C07D519/00

Abstract: The present invention provides Pyrazolopyrimidine Compounds of Formula (I): wherein L, T, Z, U, V, W, R3, R6, R7, R8, and m are as defined herein, and pharmaceutically acceptable salts of such Pyrazolopyrimidine Compounds. The Pyrazolopyrimidine Compounds are useful in the treatment of cancer and other diseases or disorders wherein mTOR is deregulated.

Abstract translation: 本发明提供式（I）的吡唑并嘧啶化合物：其中L，T，Z，U，V，W，R 3，R 6，R 7，R 8和m如本文所定义，以及这些吡唑并嘧啶化合物的药学上可接受的盐。 吡唑并嘧啶化合物可用于治疗其中mTOR失调的癌症和其它疾病或病症。

公开(公告)号：US20100298314A1

公开(公告)日：2010-11-25

申请号：US12519733

申请日：2007-12-17

Applicant: Panduranga Adulla P. Reddy ,  M. Arshad Siddiqui ,  Praveen K. Tadikonda ,  Umar Faruk Mansoor ,  Gerald W. Shipps, JR. ,  David B. Belanger ,  Lianyun Zhao

Inventor： Panduranga Adulla P. Reddy ,  M. Arshad Siddiqui ,  Praveen K. Tadikonda ,  Umar Faruk Mansoor ,  Gerald W. Shipps, JR. ,  David B. Belanger ,  Lianyun Zhao

IPC: A61K31/5377 ,  C07D471/04 ,  A61K31/437 ,  A61K31/496 ,  A61K31/497 ,  A61K31/519 ,  A61K31/4985 ,  A61P29/00 ,  A61P19/02 ,  A61P11/06 ,  A61P17/06 ,  A61P3/10 ,  A61P9/00 ,  A61P37/00

CPC classification number: C07D471/04 ,  C07D487/04

Abstract: Disclosed are substituted imidazo[1,2-a]pyridines, imidazo[1,2-a]pyrazines, imidazo[1,2-c]pyrimidines and imidazo[1,2-d]triazines compounds of the formula: (1.0) Also disclosed are methods for treating JNK1 and ERK mediated diseases using the compounds of formula 1.0.

Abstract translation: 公开了下式的取代咪唑并[1,2-a]吡啶，咪唑并[1,2-a]吡嗪，咪唑并[1,2-c]嘧啶和咪唑并[1,2-d]三嗪化合物：（1.0） 还公开了使用式1.0化合物治疗JNK1和ERK介导的疾病的方法。

公开(公告)号：US20090175852A1

公开(公告)日：2009-07-09

申请号：US12362367

申请日：2009-01-29

Applicant: Jeffrey P. Ciavarri ,  Panduranga Adulla P. Reddy ,  M. Arshad Siddiqui ,  Lianyun Zhao

Inventor： Jeffrey P. Ciavarri ,  Panduranga Adulla P. Reddy ,  M. Arshad Siddiqui ,  Lianyun Zhao

IPC: A61K31/4985 ,  C07D487/04 ,  A61K39/395 ,  A61P35/00

CPC classification number: C07D487/04

Abstract: In its many embodiments, the present invention provides a novel class of imidazopyrazine compounds as inhibitors of protein and/or checkpoint kinases, methods of preparing such compounds, pharmaceutical compositions including one or more such compounds, methods of preparing pharmaceutical formulations including one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the protein or checkpoint kinases using such compounds or pharmaceutical compositions.

Abstract translation: 在其许多实施方案中，本发明提供了一类新颖的咪唑并吡嗪化合物作为蛋白质和/或检查点激酶的抑制剂，制备此类化合物的方法，包含一种或多种此类化合物的药物组合物，制备药物制剂的方法，包括一种或多种 化合物，以及使用这些化合物或药物组合物治疗，预防，抑制或改善与蛋白质或检查点激酶相关的一种或多种疾病的方法。

公开(公告)号：US20230139282A1

公开(公告)日：2023-05-04

申请号：US17795349

申请日：2021-02-02

Applicant: Manuel DE LERA RUIZ ,  Paola FAVUZZA ,  Zhuyan GUO ,  Bin HU ,  Michael J. KELLY, III ,  Zhiyu LEI ,  John A. MCCAULEY ,  David B. OLSEN ,  Brad SLEEBS ,  Tony TRIGLIA ,  Dongmei ZHAN ,  Lianyun ZHAO ,  Merck Sharp & Dohme LLC ,  The Walter and Eliza Hall Institute of Medical Research ,  MSD R&D (China) Co., Ltd.

Inventor： Manuel de Lera Ruiz ,  Paola Favuzza ,  Zhuyan Guo ,  Bin Hu ,  Michael J. Kelly, III ,  Zhiyu Lei ,  John A. McCauley ,  David B. Olsen ,  Brad Sleebs ,  Tony Triglia ,  Dongmei Zhan ,  Lianyun Zhao

IPC: A61K31/513 ,  A61K45/06 ,  C07D405/12 ,  C07D233/88 ,  C07D405/14 ,  C07D417/14 ,  C07D491/18 ,  A61P33/06 ,  A61K31/529 ,  A61K31/5377 ,  C07D401/06

Abstract: Provided are methods of treating malaria comprising administration of compounds of Formula (I) or a pharmaceutically acceptable salt thereof, to a subject in need thereof, wherein the variables are as defined herein. Also provided are uses of the compounds of Formula (I), as defined herein, for treating a Plasmodium infection, and for treating malaria. Also provided are methods of treatment further comprising administration of one or more additional anti-malarial compounds.

公开(公告)号：US08703784B2

公开(公告)日：2014-04-22

申请号：US13818153

申请日：2011-08-22

Applicant: Zhaoyang Meng ,  Panduranga Adulla P. Reddy ,  M. Arshad Siddiqui ,  Amit K. Mandal ,  Duan Liu ,  Lianyun Zhao ,  Andrew McRiner

Inventor： Zhaoyang Meng ,  Panduranga Adulla P. Reddy ,  M. Arshad Siddiqui ,  Amit K. Mandal ,  Duan Liu ,  Lianyun Zhao ,  Andrew McRiner

IPC: A61K31/505

CPC classification number: C07D471/14 ,  C07D498/08 ,  C07D519/00

Abstract: This invention relates to novel fused tricyclic compounds under Formula I that are inhibitors of mammalian Target of Rapamycin (mTOR) kinase, which is also known as FRAP, RAFT, RAPT or SEP, and are useful in the treatment of cellular proliferative diseases, for example cancer and other proliferative disorders.

Abstract translation: 本发明涉及式I下的新型稠合三环化合物，其是哺乳动物雷帕霉素靶标（mTOR）激酶的抑制剂，其也称为FRAP，RAFT，RAPT或SEP，并且可用于治疗细胞增殖性疾病，例如 癌症和其他增殖性疾病。

公开(公告)号：US08609675B2

公开(公告)日：2013-12-17

申请号：US13379685

申请日：2010-06-30

Applicant: Cliff C. Cheng ,  Hongbo Zeng ,  Gerald W. Shipps, Jr. ,  Yongqi Deng ,  Zhaoyang Meng ,  Lianyun Zhao ,  Yang Nan ,  Binyuan Sun ,  Duan Liu ,  Panduranga A. Reddy ,  M. Arshad Siddiqui

Inventor： Cliff C. Cheng ,  Hongbo Zeng ,  Gerald W. Shipps, Jr. ,  Yongqi Deng ,  Zhaoyang Meng ,  Lianyun Zhao ,  Yang Nan ,  Binyuan Sun ,  Duan Liu ,  Panduranga A. Reddy ,  M. Arshad Siddiqui

IPC: A01N43/54 ,  C07D491/00

CPC classification number: C07D487/14

Abstract: The present invention provides Fused Tricyclic Compounds of the Formula (I) wherein Q, R1, R2, R3, and R4 are as defined herein, and pharmaceutically acceptable salts of such Fused Tricyclic Compounds. The Fused Tricyclic Compounds are useful in the treatment of cancer and other proliferative disorders.

Abstract translation: 本发明提供了其中Q，R 1，R 2，R 3和R 4如本文所定义的式（I）的稠合三环化合物和这种稠合三环化合物的药学上可接受的盐。 融合的三环化合物可用于治疗癌症和其他增殖性疾病。

公开(公告)号：US07576085B2

公开(公告)日：2009-08-18

申请号：US11272392

申请日：2005-11-10

Applicant: Timothy J. Guzi ,  Kamil Paruch ,  Michael P. Dwyer ,  Lianyun Zhao ,  Patrick J. Curran ,  David B. Belanger ,  Blake Hamann ,  Panduranga A. Reddy ,  M. Arshad Siddiqui

Inventor： Timothy J. Guzi ,  Kamil Paruch ,  Michael P. Dwyer ,  Lianyun Zhao ,  Patrick J. Curran ,  David B. Belanger ,  Blake Hamann ,  Panduranga A. Reddy ,  M. Arshad Siddiqui

IPC: A01N43/58 ,  A01N43/60 ,  A61K31/50 ,  A61K31/495 ,  C07D403/00 ,  C07D471/00 ,  C07D487/00 ,  C07D491/00 ,  C07D495/00 ,  C07D497/00

CPC classification number: C07D487/04

Abstract: In its many embodiments, the present invention provides a novel class of imidazo[1,2-a]pyrazine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions. An illustrative compound of the invention is shown below:

Abstract translation: 在其许多实施方案中，本发明提供了一类新颖的咪唑并[1,2-a]吡嗪化合物作为细胞周期蛋白依赖性激酶的抑制剂，制备此类化合物的方法，含有一种或多种此类化合物的药物组合物，制备药物制剂的方法 包括一种或多种这样的化合物，以及使用这些化合物或药物组合物治疗，预防，抑制或改善与CDK相关的一种或多种疾病的方法。 本发明的说明性化合物如下所示：