公开(公告)号：WO2017059702A1

公开(公告)日：2017-04-13

申请号：PCT/CN2016/087857

申请日：2016-06-30

Applicant: ACEA BIOSCIENCES, INC ,  ACEA PHARMACEUTICAL RESEARCH CO., LTD.

Inventor： MAO, Long ,  LIU, Jia ,  CHEN, Yile ,  HUA, Yuning ,  DAI, Kongen ,  BAO, Yimei ,  WENG, Bojie ,  MO, Xiaopeng ,  WU, Jian ,  XU, Xiao ,  XU, Wanhong ,  WANG, Xiaobo

IPC: A61K31/52 ,  C07D487/04 ,  A61P35/00

CPC classification number: A61K31/52 ,  C07D487/04

Abstract: Provided are methods of making certain pyrrolopyrimidine derivatives, which are useful in the treatment of proliferation disorders and other diseases related to the dysregulation of kinase (such as, but not limited to, EGFR (including HER), Alk, PDGFR, BLK, BMX/ETK, BTK, FLT3 (D835Y), ITK, JAK1, JAK2, JAK3, TEC and TXK) and/or the respective pathways, salts, polymorphs, and amorphous forms of said compounds, synthetic intermediates for preparing said compounds, and pharmaceutical compositions comprising said compounds and methods for making such compositions.

Abstract translation: 提供制备某些吡咯并嘧啶衍生物的方法，其可用于治疗与激酶失调相关的增殖障碍和其它疾病（例如但不限于EGFR（包括HER），Alk，PDGFR，BLK，BMX / ETK，BTK，FLT3（D835Y），ITK，JAK1，JAK2，JAK3，TEC和TXK）和/或所述化合物的相应途径，盐，多晶型物和无定形形式，用于制备所述化合物的合成中间体和包含 所述化合物和制备这种组合物的方法。

公开(公告)号：WO2020029156A1

公开(公告)日：2020-02-13

申请号：PCT/CN2018/099535

申请日：2018-08-09

Applicant: ACEA THERAPEUTICS, INC. ,  HANGZHOU ACEA PHARMACEUTICAL RESEARCH CO., LTD. ,  ZHEJIANG ACEA PHARMACEUTICALS CO., LTD

Inventor： MAO, Long ,  LIU, Jia ,  CHEN, Yile ,  HUA, Yuning ,  DONG, Kunhua ,  CHEN, Liang ,  WENG, Bojie ,  MO, Xiaopeng ,  DAI, Kongen ,  BAO, Yimei ,  WU, Jian ,  LIANG, Bin ,  ZHOU, Guanglin ,  WANG, Zhen

IPC: C07D239/47 ,  A61K31/505 ,  A61P35/00

Abstract: The invention relates to solid forms of certain N-(pyrimidinyloxy)acrylamide derivatives that are useful in the treatment of proliferation and immunological disorders and other diseases related to the dysregulation of kinases including EGFR (including HER), Alk, PDGFR, BLK, BMX/ETK, BTK, FLT3 (D835Y), ITK, JAK1, JAK2, JAK3, TEC and TXK. The invention provides methods of making these materials and their salts and polymorphs, and intermediates for preparing these materials, as well as pharmaceutical compositions comprising these materials. The solid forms and pharmaceutical compositions comprising them are useful to treat conditions including a proliferation disorder, a tumor, an inflammatory disease, an autoimmune disease, psoriasis, dry eye, rheumatoid arthritis, or lupus.

公开(公告)号：WO2023287783A1

公开(公告)日：2023-01-19

申请号：PCT/US2022/036815

申请日：2022-07-12

Applicant: ACEA THERAPEUTICS, INC. ,  HANGZHOU ACEA PHARMACEUTICAL RESEARCH CO., LTD.

Inventor： MAO, Long ,  TANG, Wei ,  ZHANG, Xiaoying ,  XU, Rongda ,  CHEN, Yile ,  XU, Xiao ,  XU, Changxu

IPC: A61P35/00 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D487/04 ,  C07D491/048 ,  C07D491/052 ,  A61K31/506 ,  A61K31/513 ,  A61K31/519

Abstract: The present disclosure relates to pharmaceutical compounds, compositions and methods, especially as they are related to compositions and methods comprising a compound of any one of Formulas (I), (II), (III), and (IV) as further described herein. The compounds are inhibitors of protein kinases associated with cancers, and are thus useful for the treatment and/or prevention of a tumor or cancer.

公开(公告)号：US20250136576A1

公开(公告)日：2025-05-01

申请号：US18578240

申请日：2022-07-12

Applicant: ACEA Therapeutics, Inc. ,  Hangzhou ACEA Pharmaceutical Research Co., Ltd.

Inventor： Long Mao ,  Wei Tang ,  Xiaoying Zhang ,  Rongda Xu ,  Yile Chen ,  Xiao Xu ,  Changxu Xu

IPC: C07D401/12 ,  C07D471/04 ,  C07D491/048

Abstract: The present disclosure relates to pharmaceutical compounds, compositions and methods, especially as they are related to compositions and methods comprising a compound of any one of Formulas (I), (II), (III), and (IV) as further described herein. The compounds are inhibitors of protein kinases associated with cancers, and are thus useful for the treatment and/or prevention of a tumor or cancer.

公开(公告)号：US20210300931A1

公开(公告)日：2021-09-30

申请号：US16500384

申请日：2017-04-07

Applicant: ACEA Therapeutics, Inc. ,  Hangzhou ACEA Pharmaceutical Research Co., Ltd. ,  Zhejiang ACEA Pharmaceuticals Co., Ltd.

Inventor： Long MAO ,  Jia LIU ,  Yile CHEN ,  Yuning HUA ,  Kongen DAI ,  Yimei BAO ,  Bojie WENG ,  Xi-aopeng MO ,  Jian WU ,  Xiao XU ,  Wanhong XU ,  Xiaobo WANG

IPC: C07D487/04 ,  A61K9/20 ,  A61K9/00

Abstract: Disclosed methods of making certain pyrrolopyrimidine derivatives, which are useful in the treatment of proliferation disorders and other diseases related to the dysregulation of kinase (such as, but not limited to, EGFR (including HER), Alk, PDGFR, BLK, BMX/ETK, BTK, FLT3(D835Y), ITK, JAK1, JAK2, JAK3, TEC AND TXK) and/or the respective pathways, salts, polymorphs, and amorphous forms of said compounds, synthetic intermediates for preparing said compounds, and pharmaceutical compositions comprising said compounds and methods for making such compositions.

公开(公告)号：US11498922B2

公开(公告)日：2022-11-15

申请号：US16500384

申请日：2017-04-07

Applicant: ACEA Therapeutics, Inc. ,  Hangzhou ACEA Pharmaceutical Research Co., Ltd. ,  Zhejiang ACEA Pharmaceuticals Co., Ltd

Inventor： Long Mao ,  Jia Liu ,  Yile Chen ,  Yuning Hua ,  Kongen Dai ,  Yimei Bao ,  Bojie Weng ,  Xi-aopeng Mo ,  Jian Wu ,  Xiao Xu ,  Wanhong Xu ,  Xiaobo Wang

IPC: A61K31/519 ,  C07D487/04 ,  A61K9/00 ,  A61K9/20

Abstract: The present invention relates to methods of making certain pyrrolopyrimidine derivatives, which are useful in the treatment of proliferation disorders and other diseases related to the dysregulation of kinase (such as, but not limited to, EGFR (including HER), Alk, PDGFR, BLK, BMX/ETK, BTK, FLT3(D835Y), ITK, JAK1, JAK2, JAK3, TEC and TXK) and/or the respective pathways, salts, polymorphs, and amorphous forms of said compounds, synthetic intermediates for preparing said compounds, and pharmaceutical compositions comprising said compounds and methods for making such compositions.

公开(公告)号：US20210309642A1

公开(公告)日：2021-10-07

申请号：US17266075

申请日：2018-08-09

Applicant: ACEA Therapeutics, Inc. ,  HANGZHOU ACEA PHARMACEUTICAL RESEARCH CO., LTD ,  ZHEJIANG ACEA PHARMACEUTICALS CO., LTD.

Inventor： Long MAO ,  Jia LIU ,  Yile CHEN ,  Yuning HUA ,  Kunhua DONG ,  Liang CHEN ,  Bojie WENG ,  Xiaopeng MO ,  Kongen DAI ,  Yimei BAO ,  Jian WU ,  Bin LIANG ,  Guanglin ZHOU ,  Zhen WANG

IPC: C07D403/12 ,  A61K9/48 ,  A61K9/20 ,  A61K9/28

Abstract: The invention relates to solid forms of certain N-(pyrimidinyloxy)acrylamide derivatives that are useful in the treatment of proliferation and immunological disorders and other diseases related to the dysregulation of kinases including EGFR (including HER), Alk, PDGFR, BLK, BMX/ETK, BTK, FLT3 (D835Y), ITK, JAK1, JAK2, JAK3, TEC and TXK. The invention provides methods of making these materials and their salts and polymorphs, and intermediates for preparing these materials, as well as pharmaceutical compositions comprising these materials. The solid forms and pharmaceutical compositions comprising them are useful to treat conditions including a proliferation disorder, a tumor, an inflammatory disease, an autoimmune disease, psoriasis, dry eye, rheumatoid arthritis, or lupus.

公开(公告)号：TW201722431A

公开(公告)日：2017-07-01

申请号：TW105132675

申请日：2016-10-07

Applicant: 艾森生物科學公司 ,  ACEA BIOSCIENCES, INC. ,  艾森生物(杭州)有限公司 ,  ACEA BIO (HANGZHOU) CO., LTD. ,  杭州艾森醫藥研究有限公司 ,  ACEA PHARMACEUTICAL RESEARCH CO., LTD.

Inventor： 毛 龍 ,  MAO, LONG ,  劉 佳 ,  LIU, JIA ,  陳以樂 ,  CHEN, YILE ,  華宇寧 ,  HUA, YUNING ,  代孔恩 ,  DAI, KONGEN ,  包益梅 ,  BAO, YIMEI ,  翁波杰 ,  WENG, BOJIE ,  莫小鵬 ,  MO, XIAOPENG ,  吳健 ,  WU, JIAN ,  徐曉 ,  XU, XIAO ,  徐萬紅 ,  XU, WANHONG ,  王 小波 ,  WANG, XIAOBO

IPC: A61K31/519 ,  A61K47/02 ,  A61K47/36 ,  A61K47/38

CPC classification number: A61K31/52 ,  C07D487/04

Abstract: 本發明係關於製造某些吡咯并嘧啶衍生物之方法，該等衍生物適用於治療增殖病症及與激酶(諸如(但不限於) EGFR (包括HER)、Alk、PDGFR、BLK、BMX/ETK、BTK、FLT3(D835Y)、ITK、JAK1、JAK2、JAK3、TEC及TXK)及/或對應路徑之調節異常相關之其他疾病；係關於該等化合物之鹽、多晶型物及非晶型式，用於製備該等化合物之合成中間物，及包含該等化合物之醫藥組合物以及製造此類組合物的方法。

Abstract in simplified Chinese: 本发明系关于制造某些吡咯并嘧啶衍生物之方法，该等衍生物适用于治疗增殖病症及与激酶(诸如(但不限于) EGFR (包括HER)、Alk、PDGFR、BLK、BMX/ETK、BTK、FLT3(D835Y)、ITK、JAK1、JAK2、JAK3、TEC及TXK)及/或对应路径之调节异常相关之其他疾病；系关于该等化合物之盐、多晶型物及非晶型式，用于制备该等化合物之合成中间物，及包含该等化合物之医药组合物以及制造此类组合物的方法。

公开(公告)号：AU2018436086A1

公开(公告)日：2021-02-25

申请号：AU2018436086

申请日：2018-08-09

Applicant: ACEA THERAPEUTICS INC ,  HANGZHOU ACEA PHARMACEUTICAL RESEARCH CO LTD ,  ZHEJIANG ACEA PHARMACEUTICALS CO LTD

Inventor： MAO LONG ,  LIU JIA ,  CHEN YILE ,  HUA YUNING ,  DONG KUNHUA ,  CHEN LIANG ,  WENG BOJIE ,  MO XIAOPENG ,  DAI KONGEN ,  BAO YIMEI ,  WU JIAN ,  LIANG BIN ,  ZHOU GUANGLIN ,  WANG ZHEN

IPC: C07D239/47 ,  A61K31/505 ,  A61P35/00

Abstract: The invention relates to solid forms of certain N-(pyrimidinyloxy)acrylamide derivatives that are useful in the treatment of proliferation and immunological disorders and other diseases related to the dysregulation of kinases including EGFR (including HER), Alk, PDGFR, BLK, BMX/ETK, BTK, FLT3 (D835Y), ITK, JAK1, JAK2, JAK3, TEC and TXK. The invention provides methods of making these materials and their salts and polymorphs, and intermediates for preparing these materials, as well as pharmaceutical compositions comprising these materials. The solid forms and pharmaceutical compositions comprising them are useful to treat conditions including a proliferation disorder, a tumor, an inflammatory disease, an autoimmune disease, psoriasis, dry eye, rheumatoid arthritis, or lupus.

公开(公告)号：AU2017408099A2

公开(公告)日：2019-11-14

申请号：AU2017408099

申请日：2017-04-07

Applicant: ACEA THERAPEUTICS INC ,  HANGZHOU ACEA PHARMACEUTICAL RESEARCH CO LTD ,  ZHEJIANG ACEA PHARMACEUTICALS CO LTD

Inventor： MAO LONG ,  LIU JIA ,  CHEN YILE ,  HUA YUNING ,  DAI KONGEN ,  BAO YIMEI ,  WENG BOJIE ,  MO XIAOPENG ,  WU JIAN ,  XU XIAO ,  XU WANHONG ,  WANG XIAOBO

IPC: C07D487/04 ,  A61K31/52 ,  A61P35/00

Abstract: Disclosed methods of making certain pyrrolopyrimidine derivatives, which are useful in the treatment of proliferation disorders and other diseases related to the dysregulation of kinase (such as, but not limited to, EGFR(including HER), Alk, PDGFR, BLK, BMX/ETK, BTK, FLT3(D835Y), ITK, JAK1, JAK2, JAK3, TEC AND TXK) and/or the respective pathways, salts, polymorphs, and amorphous forms of sid compounds, synthetic intermediates for preparing said compounds, and pharmaceutical compositions comprising said compounds and methods for making such compositions.