JP2011001339A5 - - Google Patents
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- JP2011001339A5 JP2011001339A5 JP2009236444A JP2009236444A JP2011001339A5 JP 2011001339 A5 JP2011001339 A5 JP 2011001339A5 JP 2009236444 A JP2009236444 A JP 2009236444A JP 2009236444 A JP2009236444 A JP 2009236444A JP 2011001339 A5 JP2011001339 A5 JP 2011001339A5
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- Prior art keywords
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- alkylamino
- salt
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- 125000001424 substituent group Chemical group 0.000 claims 60
- 150000001875 compounds Chemical class 0.000 claims 40
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 39
- 150000003839 salts Chemical class 0.000 claims 21
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims 18
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 9
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 9
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 8
- 125000004739 (C1-C6) alkylsulfonyl group Chemical group 0.000 claims 7
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical class CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 claims 7
- 108091007960 PI3Ks Proteins 0.000 claims 7
- 102000003993 Phosphatidylinositol 3-kinases Human genes 0.000 claims 7
- 108090000430 Phosphatidylinositol 3-kinases Proteins 0.000 claims 7
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 claims 7
- 125000005843 halogen group Chemical group 0.000 claims 7
- 239000004480 active ingredient Substances 0.000 claims 6
- 125000001072 heteroaryl group Chemical group 0.000 claims 6
- 125000004916 (C1-C6) alkylcarbonyl group Chemical group 0.000 claims 5
- 206010028980 Neoplasm Diseases 0.000 claims 5
- 125000003282 alkyl amino group Chemical group 0.000 claims 5
- 125000003277 amino group Chemical group 0.000 claims 5
- 125000003118 aryl group Chemical group 0.000 claims 5
- 239000003814 drug Substances 0.000 claims 5
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 4
- 102000013530 TOR Serine-Threonine Kinases Human genes 0.000 claims 4
- 108010065917 TOR Serine-Threonine Kinases Proteins 0.000 claims 4
- 229940124597 therapeutic agent Drugs 0.000 claims 4
- 239000002246 antineoplastic agent Substances 0.000 claims 3
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 3
- 125000004093 cyano group Chemical group *C#N 0.000 claims 3
- 229910052757 nitrogen Inorganic materials 0.000 claims 3
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 3
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 3
- 125000004845 (C1-C6) alkylsulfonylamino group Chemical group 0.000 claims 2
- YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical group C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 claims 2
- 102100032543 Phosphatidylinositol 3,4,5-trisphosphate 3-phosphatase and dual-specificity protein phosphatase PTEN Human genes 0.000 claims 2
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical group C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims 2
- 125000004448 alkyl carbonyl group Chemical group 0.000 claims 2
- 125000004657 aryl sulfonyl amino group Chemical group 0.000 claims 2
- 125000002393 azetidinyl group Chemical group 0.000 claims 2
- 125000005419 heteroarylsulfonylamino group Chemical group 0.000 claims 2
- 239000003112 inhibitor Substances 0.000 claims 2
- 230000035772 mutation Effects 0.000 claims 2
- 125000004043 oxo group Chemical group O=* 0.000 claims 2
- 125000004193 piperazinyl group Chemical group 0.000 claims 2
- 125000003386 piperidinyl group Chemical group 0.000 claims 2
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims 2
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims 1
- 208000003174 Brain Neoplasms Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 108010011536 PTEN Phosphohydrolase Proteins 0.000 claims 1
- 101710132081 Phosphatidylinositol 3,4,5-trisphosphate 3-phosphatase and dual-specificity protein phosphatase PTEN Proteins 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical group C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims 1
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- 208000002495 Uterine Neoplasms Diseases 0.000 claims 1
- 125000004457 alkyl amino carbonyl group Chemical group 0.000 claims 1
- 125000004471 alkyl aminosulfonyl group Chemical group 0.000 claims 1
- 125000003806 alkyl carbonyl amino group Chemical group 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 125000005129 aryl carbonyl group Chemical group 0.000 claims 1
- 125000004391 aryl sulfonyl group Chemical group 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 208000035250 cutaneous malignant susceptibility to 1 melanoma Diseases 0.000 claims 1
- 125000006254 cycloalkyl carbonyl group Chemical group 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000002485 formyl group Chemical group [H]C(*)=O 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 125000005143 heteroarylsulfonyl group Chemical group 0.000 claims 1
- 229910052739 hydrogen Inorganic materials 0.000 claims 1
- 239000001257 hydrogen Substances 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 230000002018 overexpression Effects 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 229940043441 phosphoinositide 3-kinase inhibitor Drugs 0.000 claims 1
- 230000026731 phosphorylation Effects 0.000 claims 1
- 238000006366 phosphorylation reaction Methods 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 1
- 206010046766 uterine cancer Diseases 0.000 claims 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2009236444A JP5090423B2 (ja) | 2008-10-14 | 2009-10-13 | モルホリノプリン誘導体 |
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2008264797 | 2008-10-14 | ||
| JP2008264797 | 2008-10-14 | ||
| JP2009121690 | 2009-05-20 | ||
| JP2009121690 | 2009-05-20 | ||
| JP2009236444A JP5090423B2 (ja) | 2008-10-14 | 2009-10-13 | モルホリノプリン誘導体 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2011001339A JP2011001339A (ja) | 2011-01-06 |
| JP2011001339A5 true JP2011001339A5 (enExample) | 2012-09-20 |
| JP5090423B2 JP5090423B2 (ja) | 2012-12-05 |
Family
ID=42106564
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009236444A Expired - Fee Related JP5090423B2 (ja) | 2008-10-14 | 2009-10-13 | モルホリノプリン誘導体 |
Country Status (21)
| Country | Link |
|---|---|
| US (2) | US8097622B2 (enExample) |
| EP (1) | EP2336132B1 (enExample) |
| JP (1) | JP5090423B2 (enExample) |
| KR (1) | KR101614976B1 (enExample) |
| CN (1) | CN102245607B (enExample) |
| AU (1) | AU2009304789B2 (enExample) |
| BR (1) | BRPI0920199A2 (enExample) |
| CA (1) | CA2740471C (enExample) |
| CO (1) | CO6362009A2 (enExample) |
| DK (1) | DK2336132T3 (enExample) |
| ES (1) | ES2452541T3 (enExample) |
| IL (1) | IL212278A (enExample) |
| MX (1) | MX2011003490A (enExample) |
| MY (1) | MY156456A (enExample) |
| NZ (1) | NZ592761A (enExample) |
| PL (1) | PL2336132T3 (enExample) |
| PT (1) | PT2336132E (enExample) |
| RU (1) | RU2490269C2 (enExample) |
| TW (1) | TWI378933B (enExample) |
| WO (1) | WO2010044401A1 (enExample) |
| ZA (1) | ZA201102449B (enExample) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
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| ES2533788T3 (es) * | 2008-05-30 | 2015-04-14 | Genentech, Inc. | Compuestos inhibidores de PI3K de tipo purina y métodos de uso |
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| EA026134B1 (ru) | 2010-12-16 | 2017-03-31 | Ф. Хоффманн-Ля Рош Аг | Трициклические ингибиторы pi3k и способы их применения |
| SG11201401716XA (en) | 2011-10-28 | 2014-05-29 | Novartis Ag | Novel purine derivatives and their use in the treatment of disease |
| CN103012284A (zh) * | 2012-12-26 | 2013-04-03 | 无锡捷化医药科技有限公司 | 一种2-氨基-5-溴嘧啶类化合物的制备方法 |
| TW201520215A (zh) * | 2013-05-13 | 2015-06-01 | Daiichi Sankyo Co Ltd | Ｎ－□啉基嘌呤衍生物之製造方法 |
| TW201521791A (zh) * | 2013-05-13 | 2015-06-16 | Daiichi Sankyo Co Ltd | ５－｛８－［（３ｒ）－４－乙醯基－３－甲基哌－１－基］－６－□啉－４－基－９－（２，２，２－三氟乙基）－９ｈ－嘌呤－２－基｝嘧啶－２－胺、及其藥理容許鹽之新穎結晶、及其製造方法 |
| AU2014293013A1 (en) | 2013-07-26 | 2016-03-17 | Race Oncology Ltd. | Combinatorial methods to improve the therapeutic benefit of bisantrene |
| AU2014331049B2 (en) * | 2013-10-04 | 2018-03-29 | Torqur Ag | Conformationally restricted PI3K and mTOR inhibitors |
| TR201910941T4 (tr) | 2015-03-30 | 2019-08-21 | Daiichi Sankyo Co Ltd | 6-morfolinil-2-pirazolil-9H-pürin deriveleri ve PI3K inhibitörleri olarak kullanımları. |
| WO2017136689A1 (en) * | 2016-02-05 | 2017-08-10 | Academia Sinica | Purine compounds possessing anticancer activity |
| US10722484B2 (en) | 2016-03-09 | 2020-07-28 | K-Gen, Inc. | Methods of cancer treatment |
| CA3045596C (en) | 2016-12-02 | 2022-08-23 | Daiichi Sankyo Company, Limited | Endo-.beta.-n-acetylglucosaminidase |
| EP3360865A1 (en) | 2017-02-13 | 2018-08-15 | F.I.S.- Fabbrica Italiana Sintetici S.p.A. | Process for the preparation of cyclopropyldiketopiperazines, and of a key intermediate of ds-5272 |
| TWI837231B (zh) | 2018-11-29 | 2024-04-01 | 日商第一三共股份有限公司 | 含有ｅｚｈ１／２雙重抑制劑之醫藥組合及其用途 |
| CN113368114B (zh) * | 2020-03-10 | 2022-04-22 | 四川大学 | 一种吗啉嘧啶类化合物的抗肿瘤应用 |
| JP2024511996A (ja) * | 2021-03-17 | 2024-03-18 | タンゴ セラピューティクス， インコーポレイテッド | 抗がん剤としてのプリン誘導体 |
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-
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- 2009-10-12 TW TW098134442A patent/TWI378933B/zh not_active IP Right Cessation
- 2009-10-13 EP EP09820579.2A patent/EP2336132B1/en not_active Not-in-force
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- 2009-10-13 CN CN200980151585.4A patent/CN102245607B/zh not_active Expired - Fee Related
- 2009-10-13 RU RU2011119525/04A patent/RU2490269C2/ru not_active IP Right Cessation
- 2009-10-13 MX MX2011003490A patent/MX2011003490A/es active IP Right Grant
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