JP2013528204A5 - - Google Patents
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- Publication number
- JP2013528204A5 JP2013528204A5 JP2013513758A JP2013513758A JP2013528204A5 JP 2013528204 A5 JP2013528204 A5 JP 2013528204A5 JP 2013513758 A JP2013513758 A JP 2013513758A JP 2013513758 A JP2013513758 A JP 2013513758A JP 2013528204 A5 JP2013528204 A5 JP 2013528204A5
- Authority
- JP
- Japan
- Prior art keywords
- methyl
- methylmorpholin
- methylsulfonimidoyl
- amine
- pyrimidin
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
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- 229910052739 hydrogen Inorganic materials 0.000 claims 19
- 239000001257 hydrogen Substances 0.000 claims 19
- 150000001875 compounds Chemical class 0.000 claims 16
- UFHFLCQGNIYNRP-UHFFFAOYSA-N hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 15
- 150000003839 salts Chemical class 0.000 claims 9
- 239000011780 sodium chloride Substances 0.000 claims 9
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 8
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 5
- 125000004435 hydrogen atoms Chemical group [H]* 0.000 claims 4
- 125000004429 atoms Chemical group 0.000 claims 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 2
- -1 3-methylmorpholin-4-yl Chemical group 0.000 claims 2
- 125000001153 fluoro group Chemical group F* 0.000 claims 2
- YXSYJGJKBNBZLQ-BRRNQIAESA-N 1-[4-[(3R)-3-methylmorpholin-4-yl]-6-[1-(methylsulfonimidoyl)cyclopropyl]pyrimidin-2-yl]benzimidazol-2-amine Chemical compound C[C@@H]1COCCN1C1=CC(C2(CC2)[S@](C)(=N)=O)=NC(N2C3=CC=CC=C3N=C2N)=N1 YXSYJGJKBNBZLQ-BRRNQIAESA-N 0.000 claims 1
- YXSYJGJKBNBZLQ-OSXTUODASA-N 1-[4-[(3R)-3-methylmorpholin-4-yl]-6-[1-(methylsulfonimidoyl)cyclopropyl]pyrimidin-2-yl]benzimidazol-2-amine Chemical compound C[C@@H]1COCCN1C1=CC(C2(CC2)[S@@](C)(=N)=O)=NC(N2C3=CC=CC=C3N=C2N)=N1 YXSYJGJKBNBZLQ-OSXTUODASA-N 0.000 claims 1
- WUJFVGIVMGNTPV-FZAOIFNZSA-N 4-fluoro-N-methyl-1-[4-[(3R)-3-methylmorpholin-4-yl]-6-[1-(methylsulfonimidoyl)cyclopropyl]pyrimidin-2-yl]benzimidazol-2-amine Chemical compound CNC1=NC2=C(F)C=CC=C2N1C(N=1)=NC(N2[C@@H](COCC2)C)=CC=1C1([S@@](C)(=N)=O)CC1 WUJFVGIVMGNTPV-FZAOIFNZSA-N 0.000 claims 1
- WUJFVGIVMGNTPV-RZQXLCLMSA-N 4-fluoro-N-methyl-1-[4-[(3R)-3-methylmorpholin-4-yl]-6-[1-(methylsulfonimidoyl)cyclopropyl]pyrimidin-2-yl]benzimidazol-2-amine Chemical compound CNC1=NC2=C(F)C=CC=C2N1C(N=1)=NC(N2[C@@H](COCC2)C)=CC=1C1([S@](C)(=N)=O)CC1 WUJFVGIVMGNTPV-RZQXLCLMSA-N 0.000 claims 1
- HQFFRTPOWLGAIX-FZAOIFNZSA-N 4-fluoro-N-methyl-1-[4-[(3R)-3-methylmorpholin-4-yl]-6-[2-(methylsulfonimidoyl)propan-2-yl]pyrimidin-2-yl]benzimidazol-2-amine Chemical compound CNC1=NC2=C(F)C=CC=C2N1C(N=C(C=1)C(C)(C)[S@@](C)(=N)=O)=NC=1N1CCOC[C@H]1C HQFFRTPOWLGAIX-FZAOIFNZSA-N 0.000 claims 1
- HQFFRTPOWLGAIX-RZQXLCLMSA-N 4-fluoro-N-methyl-1-[4-[(3R)-3-methylmorpholin-4-yl]-6-[2-(methylsulfonimidoyl)propan-2-yl]pyrimidin-2-yl]benzimidazol-2-amine Chemical compound CNC1=NC2=C(F)C=CC=C2N1C(N=C(C=1)C(C)(C)[S@](C)(=N)=O)=NC=1N1CCOC[C@H]1C HQFFRTPOWLGAIX-RZQXLCLMSA-N 0.000 claims 1
- IVKZEHQGPBBLPD-FZAOIFNZSA-N 5-fluoro-N-methyl-1-[4-[(3R)-3-methylmorpholin-4-yl]-6-[1-(methylsulfonimidoyl)cyclopropyl]pyrimidin-2-yl]benzimidazol-2-amine Chemical compound CNC1=NC2=CC(F)=CC=C2N1C(N=1)=NC(N2[C@@H](COCC2)C)=CC=1C1([S@@](C)(=N)=O)CC1 IVKZEHQGPBBLPD-FZAOIFNZSA-N 0.000 claims 1
- IVKZEHQGPBBLPD-RZQXLCLMSA-N 5-fluoro-N-methyl-1-[4-[(3R)-3-methylmorpholin-4-yl]-6-[1-(methylsulfonimidoyl)cyclopropyl]pyrimidin-2-yl]benzimidazol-2-amine Chemical compound CNC1=NC2=CC(F)=CC=C2N1C(N=1)=NC(N2[C@@H](COCC2)C)=CC=1C1([S@](C)(=N)=O)CC1 IVKZEHQGPBBLPD-RZQXLCLMSA-N 0.000 claims 1
- FGTJUHKILGGMAK-FZAOIFNZSA-N 5-fluoro-N-methyl-1-[4-[(3R)-3-methylmorpholin-4-yl]-6-[2-(methylsulfonimidoyl)propan-2-yl]pyrimidin-2-yl]benzimidazol-2-amine Chemical compound CNC1=NC2=CC(F)=CC=C2N1C(N=C(C=1)C(C)(C)[S@@](C)(=N)=O)=NC=1N1CCOC[C@H]1C FGTJUHKILGGMAK-FZAOIFNZSA-N 0.000 claims 1
- FGTJUHKILGGMAK-RZQXLCLMSA-N 5-fluoro-N-methyl-1-[4-[(3R)-3-methylmorpholin-4-yl]-6-[2-(methylsulfonimidoyl)propan-2-yl]pyrimidin-2-yl]benzimidazol-2-amine Chemical compound CNC1=NC2=CC(F)=CC=C2N1C(N=C(C=1)C(C)(C)[S@](C)(=N)=O)=NC=1N1CCOC[C@H]1C FGTJUHKILGGMAK-RZQXLCLMSA-N 0.000 claims 1
- AORKOLDGMLWWPG-RZQXLCLMSA-N 6-fluoro-N-methyl-1-[4-[(3R)-3-methylmorpholin-4-yl]-6-[1-(methylsulfonimidoyl)cyclopropyl]pyrimidin-2-yl]benzimidazol-2-amine Chemical compound CNC1=NC2=CC=C(F)C=C2N1C(N=1)=NC(N2[C@@H](COCC2)C)=CC=1C1([S@](C)(=N)=O)CC1 AORKOLDGMLWWPG-RZQXLCLMSA-N 0.000 claims 1
- PSIPSQLSHTYKJT-FZAOIFNZSA-N 6-fluoro-N-methyl-1-[4-[(3R)-3-methylmorpholin-4-yl]-6-[2-(methylsulfonimidoyl)propan-2-yl]pyrimidin-2-yl]benzimidazol-2-amine Chemical compound CNC1=NC2=CC=C(F)C=C2N1C(N=C(C=1)C(C)(C)[S@@](C)(=N)=O)=NC=1N1CCOC[C@H]1C PSIPSQLSHTYKJT-FZAOIFNZSA-N 0.000 claims 1
- PSIPSQLSHTYKJT-RZQXLCLMSA-N 6-fluoro-N-methyl-1-[4-[(3R)-3-methylmorpholin-4-yl]-6-[2-(methylsulfonimidoyl)propan-2-yl]pyrimidin-2-yl]benzimidazol-2-amine Chemical compound CNC1=NC2=CC=C(F)C=C2N1C(N=C(C=1)C(C)(C)[S@](C)(=N)=O)=NC=1N1CCOC[C@H]1C PSIPSQLSHTYKJT-RZQXLCLMSA-N 0.000 claims 1
- JESNSKPPMWEWAT-JKGBWWFKSA-N N-methyl-1-[4-[(3R)-3-methylmorpholin-4-yl]-6-[1-(methylsulfonimidoyl)cyclopropyl]pyrimidin-2-yl]benzimidazol-2-amine Chemical compound CNC1=NC2=CC=CC=C2N1C(N=1)=NC(N2[C@@H](COCC2)C)=CC=1C1([S@](C)(=N)=O)CC1 JESNSKPPMWEWAT-JKGBWWFKSA-N 0.000 claims 1
- JESNSKPPMWEWAT-YSVRNHBLSA-N N-methyl-1-[4-[(3R)-3-methylmorpholin-4-yl]-6-[1-(methylsulfonimidoyl)cyclopropyl]pyrimidin-2-yl]benzimidazol-2-amine Chemical compound CNC1=NC2=CC=CC=C2N1C(N=1)=NC(N2[C@@H](COCC2)C)=CC=1C1([S@@](C)(=N)=O)CC1 JESNSKPPMWEWAT-YSVRNHBLSA-N 0.000 claims 1
- LRIFUSYFLXZCKX-JKGBWWFKSA-N N-methyl-1-[4-[(3R)-3-methylmorpholin-4-yl]-6-[2-(methylsulfonimidoyl)propan-2-yl]pyrimidin-2-yl]benzimidazol-2-amine Chemical compound CNC1=NC2=CC=CC=C2N1C(N=C(C=1)C(C)(C)[S@](C)(=N)=O)=NC=1N1CCOC[C@H]1C LRIFUSYFLXZCKX-JKGBWWFKSA-N 0.000 claims 1
- LRIFUSYFLXZCKX-YSVRNHBLSA-N N-methyl-1-[4-[(3R)-3-methylmorpholin-4-yl]-6-[2-(methylsulfonimidoyl)propan-2-yl]pyrimidin-2-yl]benzimidazol-2-amine Chemical compound CNC1=NC2=CC=CC=C2N1C(N=C(C=1)C(C)(C)[S@@](C)(=N)=O)=NC=1N1CCOC[C@H]1C LRIFUSYFLXZCKX-YSVRNHBLSA-N 0.000 claims 1
- YIASZZUGUQHGBB-JTJFVBHCSA-N N-methyl-1-[4-[(3R)-3-methylmorpholin-4-yl]-6-[4-(methylsulfonimidoyl)oxan-4-yl]pyrimidin-2-yl]benzimidazol-2-amine Chemical compound CNC1=NC2=CC=CC=C2N1C(N=1)=NC(N2[C@@H](COCC2)C)=CC=1C1([S@](C)(=N)=O)CCOCC1 YIASZZUGUQHGBB-JTJFVBHCSA-N 0.000 claims 1
- YIASZZUGUQHGBB-RZCFMFBHSA-N N-methyl-1-[4-[(3R)-3-methylmorpholin-4-yl]-6-[4-(methylsulfonimidoyl)oxan-4-yl]pyrimidin-2-yl]benzimidazol-2-amine Chemical compound CNC1=NC2=CC=CC=C2N1C(N=1)=NC(N2[C@@H](COCC2)C)=CC=1C1([S@@](C)(=N)=O)CCOCC1 YIASZZUGUQHGBB-RZCFMFBHSA-N 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 102000030951 Phosphotransferases Human genes 0.000 claims 1
- 108091000081 Phosphotransferases Proteins 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 claims 1
- 230000000240 adjuvant Effects 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 239000000969 carrier Substances 0.000 claims 1
- OHUHVTCQTUDPIJ-JYCIKRDWSA-N ceralasertib Chemical compound C[C@@H]1COCCN1C1=CC(C2(CC2)[S@](C)(=N)=O)=NC(C=2C=3C=CNC=3N=CC=2)=N1 OHUHVTCQTUDPIJ-JYCIKRDWSA-N 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 125000005842 heteroatoms Chemical group 0.000 claims 1
- OOEYPUFPMHMEAP-IZPCHGGPSA-N imino-[1-[2-(1H-indol-4-yl)-6-[(3R)-3-methylmorpholin-4-yl]pyrimidin-4-yl]cyclopropyl]-methyl-oxo-$l^{6}-sulfane Chemical compound C[C@@H]1COCCN1C1=CC(C2(CC2)[S@](C)(=N)=O)=NC(C=2C=3C=CNC=3C=CC=2)=N1 OOEYPUFPMHMEAP-IZPCHGGPSA-N 0.000 claims 1
- OOEYPUFPMHMEAP-ONSXPEOJSA-N imino-[1-[2-(1H-indol-4-yl)-6-[(3R)-3-methylmorpholin-4-yl]pyrimidin-4-yl]cyclopropyl]-methyl-oxo-$l^{6}-sulfane Chemical compound C[C@@H]1COCCN1C1=CC(C2(CC2)[S@@](C)(=N)=O)=NC(C=2C=3C=CNC=3C=CC=2)=N1 OOEYPUFPMHMEAP-ONSXPEOJSA-N 0.000 claims 1
- IFKRIACODANJFM-FTDQSSOUSA-N imino-[4-[2-(1H-indol-4-yl)-6-[(3R)-3-methylmorpholin-4-yl]pyrimidin-4-yl]oxan-4-yl]-methyl-oxo-$l^{6}-sulfane Chemical compound C[C@@H]1COCCN1C1=CC(C2(CCOCC2)[S@@](C)(=N)=O)=NC(C=2C=3C=CNC=3C=CC=2)=N1 IFKRIACODANJFM-FTDQSSOUSA-N 0.000 claims 1
- OHUHVTCQTUDPIJ-MUWSIPGASA-N imino-methyl-[1-[6-[(3R)-3-methylmorpholin-4-yl]-2-(1H-pyrrolo[2,3-b]pyridin-4-yl)pyrimidin-4-yl]cyclopropyl]-oxo-$l^{6}-sulfane Chemical compound C[C@@H]1COCCN1C1=CC(C2(CC2)[S@@](C)(=N)=O)=NC(C=2C=3C=CNC=3N=CC=2)=N1 OHUHVTCQTUDPIJ-MUWSIPGASA-N 0.000 claims 1
- DTTJKLNXNZAVSM-RNHBAAACSA-N imino-methyl-[1-[6-[(3R)-3-methylmorpholin-4-yl]-2-(1H-pyrrolo[2,3-c]pyridin-4-yl)pyrimidin-4-yl]cyclopropyl]-oxo-$l^{6}-sulfane Chemical compound C[C@@H]1COCCN1C1=CC(C2(CC2)S(C)(=N)=O)=NC(C=2C=3C=CNC=3C=NC=2)=N1 DTTJKLNXNZAVSM-RNHBAAACSA-N 0.000 claims 1
- FEFZJKWFEQKDHO-KHXSAUHESA-N imino-methyl-[[6-[(3R)-3-methylmorpholin-4-yl]-2-(1H-pyrrolo[2,3-b]pyridin-4-yl)pyrimidin-4-yl]methyl]-oxo-$l^{6}-sulfane Chemical compound C[C@@H]1COCCN1C1=CC(C[S@](C)(=N)=O)=NC(C=2C=3C=CNC=3N=CC=2)=N1 FEFZJKWFEQKDHO-KHXSAUHESA-N 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 125000003386 piperidinyl group Chemical group 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 125000000246 pyrimidin-2-yl group Chemical group [H]C1=NC(*)=NC([H])=C1[H] 0.000 claims 1
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 1
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US35371310P | 2010-06-11 | 2010-06-11 | |
US61/353,713 | 2010-06-11 | ||
PCT/GB2011/051074 WO2011154737A1 (en) | 2010-06-11 | 2011-06-09 | Morpholino pyrimidines and their use in therapy |
Publications (3)
Publication Number | Publication Date |
---|---|
JP2013528204A JP2013528204A (ja) | 2013-07-08 |
JP2013528204A5 true JP2013528204A5 (US07794700-20100914-C00152.png) | 2014-07-03 |
JP5721821B2 JP5721821B2 (ja) | 2015-05-20 |
Family
ID=44168987
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2013513758A Active JP5721821B2 (ja) | 2010-06-11 | 2011-06-09 | モルホリノピリミジンおよび治療におけるそれらの使用 |
Country Status (38)
Families Citing this family (48)
Publication number | Priority date | Publication date | Assignee | Title |
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SA111320519B1 (ar) * | 2010-06-11 | 2014-07-02 | Astrazeneca Ab | مركبات بيريميدينيل للاستخدام كمثبطات atr |
KR20170016498A (ko) | 2014-06-17 | 2017-02-13 | 버텍스 파마슈티칼스 인코포레이티드 | Chk1 및 atr 저해제의 병용물을 사용하는 암의 치료 방법 |
TWI700283B (zh) | 2014-08-04 | 2020-08-01 | 德商拜耳製藥公司 | 2-(嗎啉-4-基)-1,7-萘啶 |
JP7187308B2 (ja) | 2015-09-30 | 2022-12-12 | バーテックス ファーマシューティカルズ インコーポレイテッド | Dna損傷剤とatr阻害剤との組み合わせを使用する、がんを処置するための方法 |
WO2018029117A1 (en) * | 2016-08-10 | 2018-02-15 | Rheinisch-Westfälische Technische Hochschule Aachen (RWTH) | New atr inhibitors for the use in cancer therapy |
UY37616A (es) | 2017-02-24 | 2018-09-28 | Bayer Ag | Combinación de inhibidores de quinasa atr con sal de radio-223 |
WO2018153972A1 (en) | 2017-02-24 | 2018-08-30 | Bayer Pharma Aktiengesellschaft | Combination of atr kinase inhibitors and antiandrogens |
JOP20190197A1 (ar) | 2017-02-24 | 2019-08-22 | Bayer Pharma AG | مثبط كيناز ايه تي آر للاستخدام في طريقة لعلاج مرض فرط التكاثر |
WO2018206547A1 (en) | 2017-05-12 | 2018-11-15 | Bayer Pharma Aktiengesellschaft | Combination of bub1 and atr inhibitors |
EP3630116B1 (en) | 2017-05-26 | 2024-05-01 | The Board Of Regents Of The University Of Texas System | Tetrahydropyrido[4,3-d]pyrimidine inhibitors of atr kinase |
CN117466884A (zh) | 2017-07-13 | 2024-01-30 | 德州大学系统董事会 | 用作atr激酶抑制剂的杂环化合物或其盐、包含其的药物组合物及用途 |
WO2019025440A1 (en) | 2017-08-04 | 2019-02-07 | Bayer Pharma Aktiengesellschaft | COMBINATION OF ATR KINASE INHIBITORS AND PD-1 / PD-L1 INHIBITORS |
CN111886224A (zh) * | 2017-08-17 | 2020-11-03 | 德州大学系统董事会 | Atr激酶的杂环抑制剂 |
JP7235338B2 (ja) * | 2017-09-08 | 2023-03-08 | ニューウェーブ・ファーマスーティカル・インコーポレイテッド | Atr阻害剤としての置換ピロロピリジン |
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GB201720989D0 (en) * | 2017-12-15 | 2018-01-31 | Glaxosmithkline Ip Dev Ltd | Chemical compounds |
PT3753937T (pt) * | 2018-02-07 | 2024-02-06 | Wuxi Biocity Biopharmaceutics Co Ltd | Inibidor de atr e sua aplicação |
US10894052B2 (en) | 2018-03-16 | 2021-01-19 | Board Of Regents, The University Of Texas System | Heterocyclic inhibitors of ATR kinase |
WO2020078788A1 (en) | 2018-10-16 | 2020-04-23 | Bayer Aktiengesellschaft | Combination of atr kinase inhibitors with 2,3-dihydroimidazo[1,2-c]quinazoline compounds |
EP3899004A2 (en) | 2018-12-18 | 2021-10-27 | Astrazeneca AB | Pharmaceutical process and intermediates |
JP2022532342A (ja) | 2019-05-14 | 2022-07-14 | ニューベイション・バイオ・インコーポレイテッド | 抗がん核内ホルモン受容体標的化化合物 |
GB201908536D0 (en) * | 2019-06-13 | 2019-07-31 | Glaxosmithkline Ip Dev Ltd | Compounds |
CN112142744A (zh) * | 2019-06-28 | 2020-12-29 | 上海瑛派药业有限公司 | 取代的稠合杂芳双环化合物作为激酶抑制剂及其应用 |
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US20240150333A1 (en) * | 2020-03-20 | 2024-05-09 | H. Lee Moffitt Cancer Center And Research Institute, Inc. | Taf1 inhibitors |
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KR20230039675A (ko) * | 2020-07-13 | 2023-03-21 | 베이징 타이드 파마슈티컬 코퍼레이션 리미티드 | Atr 키나제 억제제로 사용되는 피라졸로피리미딘 화합물 |
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IT202100021863A1 (it) | 2021-08-13 | 2023-02-13 | Univ Degli Studi Milano | Morfolino pirimidine per l’uso nella prevenzione e/o nel trattamento di stati di ipereccitabilità neuronale |
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