公开(公告)号：WO2018020242A1

公开(公告)日：2018-02-01

申请号：PCT/GB2017/052178

申请日：2017-07-26

申请人： ALMAC DISCOVERY LIMITED

发明人： HEWITT, Peter ,  MCFARLAND, Mary Melissa ,  ROUNTREE, James Samuel Shane ,  BURKAMP, Frank ,  BELL, Christina ,  PROCTOR, Lauren ,  HELM, Matthew Duncan ,  O'DOWD, Colin ,  HARRISON, Timothy

IPC分类号： C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D401/04 ,  C07D409/14 ,  C07D491/10 ,  A61K31/4412 ,  A61K31/4427 ,  A61K31/513 ,  A61P19/00 ,  A61P25/16 ,  A61P35/00

摘要： The present invention relates to compounds of Formula (I) that are useful as inhibitors of the activity of the ubiquitin specific protease USP19. The present invention also relates to pharmaceutical compositions comprising these compounds and to methods of using these compounds in therapy.

摘要翻译： 本发明涉及可用作泛素特异性蛋白酶USP19活性抑制剂的式（I）化合物。 本发明还涉及包含这些化合物的药物组合物以及在治疗中使用这些化合物的方法。

公开(公告)号：WO2012069852A1

公开(公告)日：2012-05-31

申请号：PCT/GB2011/052334

申请日：2011-11-25

申请人： ALMAC DISCOVERY LIMITED ,  HARRISON, Timothy ,  BURKAMP, Frank ,  JORDAN, Linda ,  BELL, Mark ,  JANSSEN, Dominic ,  MIEL, Hugues ,  MCFARLAND, Mary

发明人： HARRISON, Timothy ,  BURKAMP, Frank ,  JORDAN, Linda ,  BELL, Mark ,  JANSSEN, Dominic ,  MIEL, Hugues ,  MCFARLAND, Mary

IPC分类号： C07D241/04 ,  C07D213/76 ,  C07D403/04 ,  C07D401/04 ,  C07D239/26 ,  C07D471/04 ,  C07D471/10 ,  C07D239/34 ,  C07D487/04 ,  C07D213/24 ,  C07D239/42 ,  A61K31/4418 ,  C07D213/30 ,  C07D401/14 ,  A61K31/4427

CPC分类号： C07D241/04 ,  C07D213/24 ,  C07D213/30 ,  C07D213/76 ,  C07D239/26 ,  C07D239/34 ,  C07D239/42 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04

摘要： The present invention relates to compounds that are useful as inhibitors of the activity of one or more isoforms of sphingosine kinase. Particularly, although not exclusively, the present invention also relates to pharmaceutical compositions comprising these compounds and to the use of these compounds in the treatment and/or prevention of cancers, hyperproliferative, inflammatory, angiogenic, immune and viral infectious diseases.

摘要翻译： 本发明涉及可用作一种或多种鞘氨醇激酶同种型的活性抑制剂的化合物。 特别地，尽管不是唯一地，本发明还涉及包含这些化合物的药物组合物以及这些化合物在治疗和/或预防癌症，过度增殖，炎性，血管生成，免疫和病毒感染性疾病中的用途。

公开(公告)号：WO2018162932A1

公开(公告)日：2018-09-13

申请号：PCT/GB2018/050620

申请日：2018-03-12

申请人： ALMAC DISCOVERY LIMITED

发明人： HEWITT, Peter ,  BURKAMP, Frank ,  WILKINSON, Andrew ,  MIEL, Hugues ,  O'DOWD, Colin

IPC分类号： C07D487/04 ,  A61K31/519 ,  A61P35/00

摘要： The present invention relates to a compound that is useful as an inhibitor of the activity of Wee-1 kinase. The present invention also relates to pharmaceutical compositions comprising this compound and to methods of using this compound in the treatment of cancer and methods of treating cancer.

公开(公告)号：WO2018011570A1

公开(公告)日：2018-01-18

申请号：PCT/GB2017/052042

申请日：2017-07-12

申请人： ALMAC DISCOVERY LIMITED

发明人： BURKAMP, Frank ,  ROUNTREE, James Samuel Shane ,  TREDER, Adam Piotr

IPC分类号： C07D471/04 ,  C07D487/04 ,  A61K31/519 ,  A61P35/00

摘要： The present invention relates to compounds that are useful as inhibitors of the activity of Wee-1 kinase. The present invention also relates to pharmaceutical compositions comprising these compounds and to methods of using these compounds in the treatment of cancer and methods of treating cancer.

摘要翻译： 本发明涉及可用作Wee-1激酶活性抑制剂的化合物。 本发明还涉及包含这些化合物的药物组合物以及使用这些化合物治疗癌症和治疗癌症的方法的方法。

公开(公告)号：WO2013140189A1

公开(公告)日：2013-09-26

申请号：PCT/GB2013/050771

申请日：2013-03-25

申请人： ALMAC DISCOVERY LIMITED

发明人： HARRISON, Timothy ,  O'DOWD, Colin ,  SHEPHERD, Steven ,  TREVITT, Graham ,  ZHANG, Lixin ,  BURKAMP, Frank

IPC分类号： C07D491/048 ,  C07D495/04 ,  C07D487/04 ,  A61K31/519 ,  A61P31/00

CPC分类号： C07D495/04 ,  C07D487/04 ,  C07D491/048

摘要： The present invention relates to compounds of Formula (I) that are useful as inhibitors of the activity of one or more isoforms of the serine / threonine kinase AKT. The present invention also relates to pharmaceutical compositions comprising these compounds and to methods of using these compounds in the treatment of cancer and methods of treating cancer.

摘要翻译： 本发明涉及可用作丝氨酸/苏氨酸激酶AKT的一种或多种同工型的活性的抑制剂的式（I）化合物。 本发明还涉及包含这些化合物的药物组合物和使用这些化合物治疗癌症的方法和治疗癌症的方法。

公开(公告)号：WO2021161047A1

公开(公告)日：2021-08-19

申请号：PCT/GB2021/050360

申请日：2021-02-12

申请人： ALMAC DISCOVERY LIMITED

发明人： JACQ, Xavier ,  LOBB, Ian Thomas ,  WAPPETT, Mark ,  JURISIC, Anamarija ,  ROUNTREE, James Samuel Shane ,  HELM, Matthew Duncan

IPC分类号： A61K31/522 ,  A61K31/513 ,  A61K31/53 ,  A61K31/4025 ,  A61K31/436 ,  A61K31/4365 ,  A61K31/4375 ,  A61K31/497 ,  A61K31/498 ,  A61K39/395 ,  A61K45/06 ,  A61P35/00 ,  A61P35/04

摘要： Provided herein are treatments for cancer by inhibition of USP7 activity, for example inhibition of USP7 activity in fibroblasts, inhibition of extra-cellular matrix remodelling in the tumour microenvironment, inhibition of VEGF, inhibition of angiogenesis or metastasis, modulation of the immune system, or a combination thereof.

公开(公告)号：WO2020254640A1

公开(公告)日：2020-12-24

申请号：PCT/EP2020/067210

申请日：2020-06-19

申请人： ALMAC DISCOVERY LIMITED

发明人： COTTON, Graham ,  THOM, Jennifer ,  TRUMPER, Paul

IPC分类号： A61K47/68 ,  A61P35/00 ,  C07K16/30

摘要： The present application relates to anthracycline derivatives and their use in forming conjugates with target-binding molecules, including but not limited to antibodies. Conjugates of target-binding molecules and anthracycline derivatives are also provided. Also provided are medical uses of and pharmaceutical compositions comprising the conjugates.

公开(公告)号：WO2020115500A1

公开(公告)日：2020-06-11

申请号：PCT/GB2019/053456

申请日：2019-12-06

申请人： ALMAC DISCOVERY LIMITED

发明人： ROUNTREE, James Samuel Shane ,  HEWITT, Peter ,  MCFARLAND, Mary Melissa ,  BURKAMP, Frank ,  BELL, Christina ,  O'DOWD, Colin ,  HARRISON, Timothy ,  HELM, Matthew Duncan ,  ROZYKA, Ewelina ,  CRANSTON, Aaron ,  JACQ, Xavier ,  PROCTOR, Lauren

IPC分类号： A61K31/4545 ,  A61K31/496 ,  A61K31/513 ,  A61K31/5377 ,  A61P3/04 ,  A61P5/48 ,  A61P21/00 ,  A61P35/00

摘要： Provided are USP19 inhibitors, methods of treating obesity, metabolic syndrome and/or diabetes using the USP19 inhibitor compounds, as well as those compounds for use in methods of treating obesity, metabolic syndrome and/or diabetes. Also provided are methods of treating muscular atrophy, for example cachexia or sarcopenia with USP19 inhibitor compounds, plus those compounds for use in methods of treating muscular atrophy.

公开(公告)号：WO2019138227A1

公开(公告)日：2019-07-18

申请号：PCT/GB2019/050058

申请日：2019-01-10

申请人： ALMAC DISCOVERY LIMITED

发明人： TREDER, Adam Piotr ,  BURKAMP, Frank

IPC分类号： C07D471/04 ,  C07D519/00 ,  A61K31/519 ,  A61P35/00

CPC分类号： C07D471/04 ,  C07D519/00

摘要： Compounds that are useful as inhibitors of the activity of Wee-1 kinase are provided. Also provided are pharmaceutical compositions comprising these compounds and to methods of using these compounds in the treatment of cancer and methods of treating cancer.

公开(公告)号：WO2018109491A1

公开(公告)日：2018-06-21

申请号：PCT/GB2017/053763

申请日：2017-12-15

申请人： ALMAC DISCOVERY LIMITED

发明人： EL-HELALI, Aya ,  MCQUILLAN, Sara ,  KNIGHT, Laura ,  KENNEDY, Richard ,  MCCABE, Nuala ,  WAPPETT, Mark

IPC分类号： A61K38/17 ,  A61P35/00

CPC分类号： A61P35/00 ,  A61K38/52 ,  C07K14/4702 ,  C12N9/90 ,  C12Y502/01008

摘要： The invention relates to treatment of EMT-associated disease, and more specifically to treatment of cancer exhibiting the EMT phenotype, using the polypeptide FKBP-L and peptide fragments thereof.