公开(公告)号：WO2019123207A1

公开(公告)日：2019-06-27

申请号：PCT/IB2018/060181

申请日：2018-12-17

Applicant: PFIZER INC. ,  MERCK PATENT GMBH ,  ARRAY BIOPHARMA INC.

Inventor： BOSHOFF, Christoffel Hendrik ,  CESARI, Rossano ,  MASSACESI, Cristian ,  PATHAN, Nuzhat ,  LEE, Patrice A. ,  WINSKI, Shannon L.

IPC: A61K31/5025 ,  A61K39/00 ,  A61K45/06 ,  A61P35/00

CPC classification number: A61K45/06 ,  A61K31/5025 ,  A61K39/39558 ,  A61P35/00 ,  C07K16/2827 ,  A61K2300/00

Abstract: This invention relates to a method of treating cancer by administering a combination therapy comprising a combination of a MEK inhibitor and a PD-1 axis binding antagonist, or a combination of a MEK inhibitor and a PARP inhibitor, or a combination of a MEK inhibitor and a PD-1 axis binding antagonist and a PARP inhibitor to a patient in need thereof.

公开(公告)号：WO2019099524A1

公开(公告)日：2019-05-23

申请号：PCT/US2018/061060

申请日：2018-11-14

Applicant: MIRATI THERAPEUTICS, INC. ,  ARRAY BIOPHARMA INC.

Inventor： BLAKE, James, F. ,  BURGESS, Laurence, E. ,  CHICARELLI, Mark, Joseph ,  CHRISTENSEN, James, Gail ,  COOK, Adam ,  FELL, Jay, Bradford ,  FISCHER, John, P. ,  MARX, Matthew, Arnold ,  MEJIA, Macedonio, J. ,  SAVECHENKOV, Pavel ,  VIGERS, Guy, P.A. ,  SMITH, Christopher, Ronald ,  RODRIGUEZ, Martha, E.

IPC: C07D401/06 ,  C07D401/14

Abstract: The present invention relates to compounds that inhibit KRas G12C. In particular, the present invention relates to compounds that irreversibly inhibit the activity of KRas G12C, pharmaceutical compositions comprising the compounds and methods of use therefor.

公开(公告)号：WO2017011776A1

公开(公告)日：2017-01-19

申请号：PCT/US2016/042576

申请日：2016-07-15

Applicant: ARRAY BIOPHARMA, INC.

Inventor： ANDREWS, Steven W. ,  BLAKE, James F. ,  CHICARELLI, Mark J. ,  GOLOS, Adam ,  HAAS, Julia ,  JIANG, Yutong ,  KOLAKOWSKI, Gabrielle R.

IPC: C07D471/04 ,  A61K31/437 ,  A61P35/00 ,  A61P29/00

CPC classification number: C07D471/04 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/497 ,  A61K31/499 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/55 ,  A61K45/06 ,  C07D519/00

Abstract: Provided herein are compounds of the General Formula I: and stereoisomers and pharmaceutically acceptable salts or solvates thereof, in which A, B, D, E, X 1 , X 2 , X 3 and X 4 have the meanings given in the specification, which are inhibitors of RET kinase and are useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including diseases or disorders mediated by a RET kinase.

Abstract translation: 本文提供了通式I的化合物及其立体异构体及其药学上可接受的盐或溶剂化物，其中A，B，D，E，X 1，X 2，X 3和X 4具有说明书中给出的含义，其为RET的抑制剂 激酶，并且可用于治疗和预防可用RET激酶抑制剂治疗的疾病，包括由RET激酶介导的疾病或病症。

公开(公告)号：WO2016138458A1

公开(公告)日：2016-09-01

申请号：PCT/US2016/019904

申请日：2016-02-26

Applicant: GENENTECH, INC. ,  ARRAY BIOPHARMA INC.

Inventor： STULTS, Jeffrey ,  LINDEMANN, Christopher M. ,  SPENCER, Keith L. ,  LIU, Weidong ,  LUBACH, Joseph

IPC: C07D471/04 ,  A61K31/437 ,  A61P35/00

CPC classification number: C07D471/04 ,  A61K31/437 ,  A61K45/06

Abstract: Disclosed are crystalline forms of (R)-N-(4-(3-aminopiperidin-1-yl)-5-bromo-1H-pyrrolo[2,3-b]pyridin-3-yl)cyclopropanecarboxamide, and salts, solvates, and hydrates thereof, and pharmaceutical compositions, formulations and a process of manufacturing thereof.

Abstract translation: 公开了（R）-N-（4-（3-氨基哌啶-1-基）-5-溴-1H-吡咯并[2,3-b]吡啶-3-基）环丙烷甲酰胺和盐，溶剂化物的结晶形式 及其水合物，以及药物组合物，制剂及其制造方法。

公开(公告)号：WO2015126750A4

公开(公告)日：2015-10-29

申请号：PCT/US2015015806

申请日：2015-02-13

Applicant: ARRAY BIOPHARMA INC

Inventor： BURGESS LAURENCE E ,  CHANTRY DAVID HARRY ,  EBERHARDT CHRISTINE D

IPC: G01N33/497 ,  G01N33/50 ,  G01N33/88

CPC classification number: G01N33/84 ,  A61K31/353 ,  A61K31/47 ,  G01N33/564 ,  G01N2800/122 ,  G01N2800/52 ,  A61K2300/00

Abstract: Provided herein is the identification of biomarkers that are predictive of a patient's responsiveness to a therapy comprising treatment with a CRTh2 antagonist, such as ARRY-502. Biomarkers identified include baseline levels of the fraction exhaled nitric oxide and the percentage of eosinophil of the total lymphocyte population in peripheral blood.

Abstract translation: 本文提供了可预测患者对包括用CRTh2拮抗剂如ARRY-502进行治疗的治疗反应性的生物标志物的鉴定。 确定的生物标志物包括呼出一氧化氮的分数的基线水平和外周血中总淋巴细胞群的嗜酸性粒细胞百分比。

公开(公告)号：WO2014074940A9

公开(公告)日：2014-08-07

申请号：PCT/US2013069331

申请日：2013-11-08

Applicant: ARRAY BIOPHARMA INC ,  ASSELIN SYLVIE ,  BRETT LISA ,  CHEN YING ,  CORSON DONALD T ,  COSBIE ANDREW ,  FARRELL ROBERT ,  GUNAWARDANA INDRANI W ,  HUANG JINKUN ,  LANE JONATHAN W ,  LEI DENNIS ,  LINDEMANN CHRISTOPHER M ,  LUU VAN ,  MANNILA CORALEE G ,  MILBURN ROBERT ,  MORRISON HENRY ,  TAN HELMING ,  TEDROW JASON ,  WATSON DANIEL J

Inventor： ASSELIN SYLVIE ,  BRETT LISA ,  CHEN YING ,  CORSON DONALD T ,  COSBIE ANDREW ,  FARRELL ROBERT ,  GUNAWARDANA INDRANI W ,  HUANG JINKUN ,  LANE JONATHAN W ,  LEI DENNIS ,  LINDEMANN CHRISTOPHER M ,  LUU VAN ,  MANNILA CORALEE G ,  MILBURN ROBERT ,  MORRISON HENRY ,  TAN HELMING ,  TEDROW JASON ,  WATSON DANIEL J

IPC: C07D417/14 ,  A61K31/444 ,  A61P3/10

CPC classification number: C07D417/14 ,  C07B2200/13

Abstract: The present invention relates to crystalline polymorph forms of (1S)-1-[5-({3-[(2-methylpyridin-3-yl)oxy]-5-(pyridin-2-ylsulfanyl)pyridin-2-yl}amino)-1,2,4-thiadiazol-3-yl]ethane-1,2-diol, to pharmaceutical compositions comprising such crystalline polymorph forms, and to processes for preparing them. The invention further relates to methods of treatment of diabetes related disorders comprising administering such solid-state forms or compositions thereof to a subject, and to use of such crystalline polymorph forms in the manufacture of medicaments.

Abstract translation: 本发明涉及（1S）-1- [5 - （{3 - [（2-甲基吡啶-3-基）氧基] -5-（吡啶-2-基硫烷基）吡啶-2-基} 氨基）-1,2,4-噻二唑-3-基]乙-1,2-二醇，涉及包含此类结晶多晶型物的药物组合物，并涉及制备它们的方法。 本发明进一步涉及治疗糖尿病相关病症的方法，包括将所述固态形式或其组合物施用于受试者，并且涉及这种结晶多晶型物在制造药物中的用途。

公开(公告)号：WO2014078454A1

公开(公告)日：2014-05-22

申请号：PCT/US2013/069951

申请日：2013-11-13

Applicant: ARRAY BIOPHARMA INC. ,  ALLEN, Shelley ,  ANDREWS, Steven, Wade ,  BLAKE, James, F. ,  BRANDHUBER, Barbara, J. ,  HAAS, Julia ,  JIANG, Yutong ,  KERCHER, Timothy ,  KOLAKOWSKI, Gabrielle, R. ,  THOMAS, Allen, A. ,  WINSKI, Shannon, L.

Inventor： ALLEN, Shelley ,  ANDREWS, Steven, Wade ,  BLAKE, James, F. ,  BRANDHUBER, Barbara, J. ,  HAAS, Julia ,  JIANG, Yutong ,  KERCHER, Timothy ,  KOLAKOWSKI, Gabrielle, R. ,  THOMAS, Allen, A. ,  WINSKI, Shannon, L.

IPC: C07D401/14 ,  C07D405/14 ,  C07D231/40 ,  C07D231/54 ,  C07D401/12 ,  C07D403/02 ,  C07D403/04 ,  C07D403/14 ,  C07D405/12 ,  C07D413/12 ,  C07D453/02 ,  A61K31/4155 ,  A61K31/416 ,  A61K31/4162 ,  A61P25/00

CPC classification number: C07D491/048 ,  C07D231/40 ,  C07D231/52 ,  C07D231/54 ,  C07D231/56 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/02 ,  C07D403/04 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/14 ,  C07D413/12 ,  C07D453/02 ,  C07D471/08

Abstract: Compounds of Formula I: or stereoisomers, tautomers, or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein Ring A, Ring C and X are as defined herein, are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation/inflammatory diseases, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis and pelvic pain syndrome.

Abstract translation: 式I化合物或其立体异构体，互变异构体或其药学上可接受的盐，溶剂合物或前药，其中环A，环C和X如本文所定义，是TrkA激酶的抑制剂，并且可用于治疗可治疗的疾病 具有TrkA激酶抑制剂如疼痛，癌症，炎症/炎性疾病，神经变性疾病，某些感染性疾病，干燥综合征，子宫内膜异位症，糖尿病性周围神经病变，前列腺炎和骨盆疼痛综合征。

公开(公告)号：WO2014078331A1

公开(公告)日：2014-05-22

申请号：PCT/US2013/069750

申请日：2013-11-12

Applicant: ARRAY BIOPHARMA INC. ,  BLAKE, James F. ,  BRANDHUBER, Barbara J. ,  HAAS, Julia ,  NEWHOUSE, Brad ,  THOMAS, Allen A. ,  WINSKI, Shannon L.

Inventor： BLAKE, James F. ,  BRANDHUBER, Barbara J. ,  HAAS, Julia ,  NEWHOUSE, Brad ,  THOMAS, Allen A. ,  WINSKI, Shannon L.

IPC: C07D403/12 ,  C07D401/14 ,  C07D231/40 ,  C07D231/52 ,  C07D231/54 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D413/12 ,  C07D495/04 ,  A61K31/4155 ,  A61P35/00 ,  A61P29/00

CPC classification number: C07D231/52 ,  C07D231/38 ,  C07D231/40 ,  C07D231/54 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D413/12 ,  C07D453/02 ,  C07D495/04

Abstract: Compounds of Formula I or stereoisomers, tautomers, or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein Ring A, Ring C, X, Ra, Rb, Rc, Rd and n are as defined herein, are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation/inflammatory diseases, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis or pelvic pain syndrome.

Abstract translation: 式I或其立体异构体，互变异构体或其药学上可接受的盐，溶剂合物或前药的化合物，其中环A，环C，X，R a，R b，R c，R d和n如本文所定义，是TrkA激酶的抑制剂，并且是有用的 治疗可用TrkA激酶抑制剂如疼痛，癌症，炎症/炎性疾病，神经变性疾病，某些感染性疾病，干燥综合征，子宫内膜异位症，糖尿病性周围神经病变，前列腺炎或骨盆疼痛综合征治疗的疾病。

公开(公告)号：WO2014074940A1

公开(公告)日：2014-05-15

申请号：PCT/US2013/069331

申请日：2013-11-08

Applicant: ARRAY BIOPHARMA INC. ,  ASSELIN, Sylvie ,  BRETT, Lisa ,  CHEN, Ying ,  CORSON, Donald T. ,  COSBIE, Andrew ,  FARRELL, Robert ,  GUNAWARDANA, Indrani W. ,  HUANG, Jinkun ,  LANE, Jonathan W. ,  LEI, Dennis ,  LINDEMANN, Christopher M ,  LUU, Van ,  MANNILA, Coralee G. ,  MILBURN, Robert ,  MORRISON, Henry ,  TAN, Helming ,  TEDROW, Jason ,  WATSON, Daniel J.

Inventor： ASSELIN, Sylvie ,  BRETT, Lisa ,  CHEN, Ying ,  CORSON, Donald T. ,  COSBIE, Andrew ,  FARRELL, Robert ,  GUNAWARDANA, Indrani W. ,  HUANG, Jinkun ,  LANE, Jonathan W. ,  LEI, Dennis ,  LINDEMANN, Christopher M ,  LUU, Van ,  MANNILA, Coralee G. ,  MILBURN, Robert ,  MORRISON, Henry ,  TAN, Helming ,  TEDROW, Jason ,  WATSON, Daniel J.

IPC: C07D417/14 ,  A61K31/444 ,  A61P3/10

CPC classification number: C07D417/14 ,  C07B2200/13

Abstract: The present invention relates to crystalline polymorph forms of (1S)-1-[5-({3-[(2-methylpyridin-3-yl)oxy]-5-(pyridin-2-ylsulfanyl)pyridin-2-yl}amino)-1,2,4-thiadiazol-3-yl]ethane-1,2-diol, to pharmaceutical compositions comprising such crystalline polymorph forms, and to processes for preparing them. The invention further relates to methods of treatment of diabetes related disorders comprising administering such solid-state forms or compositions thereof to a subject, and to use of such crystalline polymorph forms in the manufacture of medicaments.

Abstract translation: 本发明涉及（1S）-1- [5 - （{3 - [（2-甲基吡啶-3-基）氧基] -5-（吡啶-2-基硫烷基）吡啶-2-基} 氨基）-1,2,4-噻二唑-3-基]乙烷-1,2-二醇，包括这种结晶多晶型物的药物组合物及其制备方法。 本发明还涉及治疗糖尿病相关病症的方法，包括将这种固态形式或其组合物施用于受试者，以及在制备药物中使用这种结晶多晶型物。

公开(公告)号：WO2013074641A1

公开(公告)日：2013-05-23

申请号：PCT/US2012/065036

申请日：2012-11-14

Applicant: ARRAY BIOPHARMA INC. ,  FELL, Jay Bradford ,  FISCHER, John P. ,  HINKLIN, Ronald J.

Inventor： FELL, Jay Bradford ,  FISCHER, John P. ,  HINKLIN, Ronald J.

IPC: C07D401/04 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14 ,  A61K31/454 ,  A61K31/4545 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10

CPC classification number: C07D417/14 ,  C07D401/04 ,  C07D401/14 ,  C07D413/14

Abstract: Compounds of Formula I: and pharmaceutically acceptable salts thereof, in which X 1 , X 2 , R 3 , R 4 , R 5 , R x , R 7 , R 9 , R 10 and n have the meanings given in the specification, are modulators of GPR119 and are useful in the treatment or prevention of diseases such as such as, but not limited to, type 2 diabetes, diabetic complications, symptoms of diabetes, metabolic syndrome, obesity, dyslipidemia, and related conditions.

Abstract translation: 其中X1，X2，R3，R4，R5，Rx，R7，R9，R10和n具有本说明书中给出的含义的式I化合物及其药学上可接受的盐是GPR119的调节剂，可用于治疗 或预防诸如但不限于2型糖尿病，糖尿病并发症，糖尿病症状，代谢综合征，肥胖症，血脂异常和相关病症等疾病。