JP2010532387A5 - - Google Patents
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- JP2010532387A5 JP2010532387A5 JP2010515270A JP2010515270A JP2010532387A5 JP 2010532387 A5 JP2010532387 A5 JP 2010532387A5 JP 2010515270 A JP2010515270 A JP 2010515270A JP 2010515270 A JP2010515270 A JP 2010515270A JP 2010532387 A5 JP2010532387 A5 JP 2010532387A5
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- Prior art keywords
- alkyl
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- 150000001875 compounds Chemical class 0.000 claims description 103
- 229910052736 halogen Inorganic materials 0.000 claims description 16
- 125000000623 heterocyclic group Chemical group 0.000 claims description 16
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 14
- 125000004429 atom Chemical group 0.000 claims description 13
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims description 12
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 12
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 12
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 10
- 201000010099 disease Diseases 0.000 claims description 10
- 150000002367 halogens Chemical class 0.000 claims description 10
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 8
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims description 8
- 125000004186 cyclopropylmethyl group Chemical group [H]C([H])(*)C1([H])C([H])([H])C1([H])[H] 0.000 claims description 8
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 8
- 229910052739 hydrogen Inorganic materials 0.000 claims description 8
- 239000001257 hydrogen Substances 0.000 claims description 8
- 230000001404 mediated effect Effects 0.000 claims description 8
- 229910052757 nitrogen Inorganic materials 0.000 claims description 8
- 239000008194 pharmaceutical composition Substances 0.000 claims description 8
- 125000006239 protecting group Chemical group 0.000 claims description 8
- 238000000034 method Methods 0.000 claims description 7
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 7
- -1 CH 2 F Chemical compound 0.000 claims description 6
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 6
- 241000124008 Mammalia Species 0.000 claims description 6
- 238000010511 deprotection reaction Methods 0.000 claims description 6
- 229910052731 fluorine Inorganic materials 0.000 claims description 6
- 238000007306 functionalization reaction Methods 0.000 claims description 6
- 125000005843 halogen group Chemical group 0.000 claims description 6
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 6
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 4
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims description 4
- 208000035475 disorder Diseases 0.000 claims description 4
- 239000003814 drug Substances 0.000 claims description 4
- 125000002883 imidazolyl group Chemical group 0.000 claims description 4
- 238000004519 manufacturing process Methods 0.000 claims description 4
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 4
- 125000003566 oxetanyl group Chemical group 0.000 claims description 4
- 125000003386 piperidinyl group Chemical group 0.000 claims description 4
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims description 4
- 150000003839 salts Chemical class 0.000 claims description 4
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims description 4
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims description 4
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 claims description 4
- 229920002554 vinyl polymer Polymers 0.000 claims description 4
- 125000004201 2,4-dichlorophenyl group Chemical group [H]C1=C([H])C(*)=C(Cl)C([H])=C1Cl 0.000 claims description 2
- 125000004189 3,4-dichlorophenyl group Chemical group [H]C1=C([H])C(Cl)=C(Cl)C([H])=C1* 0.000 claims description 2
- 125000004800 4-bromophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Br 0.000 claims description 2
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 claims description 2
- 125000006306 4-iodophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1I 0.000 claims description 2
- 125000004864 4-thiomethylphenyl group Chemical group 0.000 claims description 2
- 125000004863 4-trifluoromethoxyphenyl group Chemical group [H]C1=C([H])C(OC(F)(F)F)=C([H])C([H])=C1* 0.000 claims description 2
- 125000004199 4-trifluoromethylphenyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)C(F)(F)F 0.000 claims description 2
- 208000024172 Cardiovascular disease Diseases 0.000 claims description 2
- 229910052794 bromium Inorganic materials 0.000 claims description 2
- 229910052801 chlorine Inorganic materials 0.000 claims description 2
- 150000002431 hydrogen Chemical class 0.000 claims description 2
- 230000003463 hyperproliferative effect Effects 0.000 claims description 2
- 208000027866 inflammatory disease Diseases 0.000 claims description 2
- 230000002401 inhibitory effect Effects 0.000 claims description 2
- 229910052740 iodine Inorganic materials 0.000 claims description 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 2
- MOZRQQTUYAYCQT-FQEVSTJZSA-N n-[[(3s)-3-amino-1-(5-ethyl-7h-pyrrolo[2,3-d]pyrimidin-4-yl)pyrrolidin-3-yl]methyl]-2,4-difluorobenzamide Chemical group C([C@]1(CCN(C1)C=1N=CN=C2NC=C(C=12)CC)N)NC(=O)C1=CC=C(F)C=C1F MOZRQQTUYAYCQT-FQEVSTJZSA-N 0.000 claims description 2
- 230000004770 neurodegeneration Effects 0.000 claims description 2
- 208000015122 neurodegenerative disease Diseases 0.000 claims description 2
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 claims description 2
- RLOWWWKZYUNIDI-UHFFFAOYSA-N phosphinic chloride Chemical compound ClP=O RLOWWWKZYUNIDI-UHFFFAOYSA-N 0.000 claims description 2
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims 5
- 125000002757 morpholinyl group Chemical group 0.000 claims 2
- 125000000217 alkyl group Chemical group 0.000 description 12
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US94814707P | 2007-07-05 | 2007-07-05 | |
| US60/948,147 | 2007-07-05 | ||
| PCT/US2008/069147 WO2009006569A1 (en) | 2007-07-05 | 2008-07-03 | Pyrimidyl cyclopentanes as akt protein kinase inhibitors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013249824A Division JP2014040489A (ja) | 2007-07-05 | 2013-12-03 | Ａｋｔプロテインキナーゼ阻害剤としてのピリミジルシクロペンタン |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2010532387A JP2010532387A (ja) | 2010-10-07 |
| JP2010532387A5 true JP2010532387A5 (cg-RX-API-DMAC7.html) | 2012-07-26 |
| JP5542282B2 JP5542282B2 (ja) | 2014-07-09 |
Family
ID=39830222
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010515270A Active JP5542282B2 (ja) | 2007-07-05 | 2008-07-03 | Ａｋｔプロテインキナーゼ阻害剤としてのピリミジルシクロペンタン |
| JP2013249824A Withdrawn JP2014040489A (ja) | 2007-07-05 | 2013-12-03 | Ａｋｔプロテインキナーゼ阻害剤としてのピリミジルシクロペンタン |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013249824A Withdrawn JP2014040489A (ja) | 2007-07-05 | 2013-12-03 | Ａｋｔプロテインキナーゼ阻害剤としてのピリミジルシクロペンタン |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US8377937B2 (cg-RX-API-DMAC7.html) |
| EP (2) | EP2173723B3 (cg-RX-API-DMAC7.html) |
| JP (2) | JP5542282B2 (cg-RX-API-DMAC7.html) |
| KR (2) | KR101624361B1 (cg-RX-API-DMAC7.html) |
| CN (1) | CN101918373B (cg-RX-API-DMAC7.html) |
| AT (1) | ATE522509T1 (cg-RX-API-DMAC7.html) |
| AU (1) | AU2008272832B2 (cg-RX-API-DMAC7.html) |
| BR (1) | BRPI0813993A2 (cg-RX-API-DMAC7.html) |
| CA (1) | CA2692506C (cg-RX-API-DMAC7.html) |
| ES (1) | ES2533557T3 (cg-RX-API-DMAC7.html) |
| IL (1) | IL202617A0 (cg-RX-API-DMAC7.html) |
| MX (1) | MX2009014013A (cg-RX-API-DMAC7.html) |
| SI (1) | SI2173723T1 (cg-RX-API-DMAC7.html) |
| WO (1) | WO2009006569A1 (cg-RX-API-DMAC7.html) |
| ZA (1) | ZA200908901B (cg-RX-API-DMAC7.html) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20150089099A (ko) * | 2007-07-05 | 2015-08-04 | 어레이 바이오파마 인크. | Ａｋｔ 단백질 키나제 억제제로서의 피리미딜 시클로펜탄 |
| US8846683B2 (en) | 2007-07-05 | 2014-09-30 | Array Biopharma, Inc. | Pyrimidyl cyclopentanes as Akt protein kinase inhibitors |
| US9409886B2 (en) | 2007-07-05 | 2016-08-09 | Array Biopharma Inc. | Pyrimidyl cyclopentanes as AKT protein kinase inhibitors |
| WO2009089352A1 (en) | 2008-01-08 | 2009-07-16 | Array Biopharma Inc. | Pyrrolopyridines as kinase inhibitors |
| JP5635910B2 (ja) | 2008-01-09 | 2014-12-03 | アレイ バイオファーマ、インコーポレイテッド | ＡＫＴタンパク質キナーゼ阻害剤としての５Ｈ−シクロペンタ［ｄ］ピリミジン |
| JP5539225B2 (ja) | 2008-01-09 | 2014-07-02 | アレイ バイオファーマ、インコーポレイテッド | Ａｋｔタンパク質キナーゼ阻害剤としての水酸化されたピリミジルシクロペンタン |
| US8372842B2 (en) | 2008-01-09 | 2013-02-12 | Array Biopharma Inc. | Pyrazolopyridines as kinase inhibitors |
| GB201110546D0 (en) * | 2011-06-22 | 2011-08-03 | Imp Innovations Ltd | Compositions |
| JP6214636B2 (ja) * | 2012-05-17 | 2017-10-18 | アレイ バイオファーマ、インコーポレイテッド | ヒドロキシル化シクロペンチルピリミジン化合物を作製するためのプロセス |
| US10722484B2 (en) | 2016-03-09 | 2020-07-28 | K-Gen, Inc. | Methods of cancer treatment |
| SG10202104386UA (en) | 2016-10-28 | 2021-05-28 | Icahn School Med Mount Sinai | Compositions and methods for treating ezh2-mediated cancer |
| JP2020514252A (ja) | 2016-12-08 | 2020-05-21 | アイカーン スクール オブ メディスン アット マウント シナイ | Ｃｄｋ４／６媒介性がんを治療するための組成物および方法 |
| CA3092677A1 (en) * | 2018-03-06 | 2019-09-12 | Icahn School Of Medicine At Mount Sinai | Serine threonine kinase (akt) degradation / disruption compounds and methods of use |
| CN112996518A (zh) | 2018-06-21 | 2021-06-18 | 西奈山伊坎医学院 | Wd40重复结构域蛋白5(wdr5)降解/破坏化合物和使用方法 |
| EP3965824B1 (en) | 2019-05-06 | 2025-01-08 | Icahn School of Medicine at Mount Sinai | Heterobifunctional compounds as degraders of hpk1 |
| BR112022017856A2 (pt) * | 2020-03-17 | 2022-11-01 | Jiangsu Hengrui Pharmaceuticals Co Ltd | Derivado bicíclico fundido, método de preparação do mesmo e uso farmacêutico do mesmo |
| CN113444110B (zh) * | 2020-03-25 | 2023-05-12 | 江苏恒瑞医药股份有限公司 | 四氢吡咯并吡唑类衍生物、其制备方法及其在医药上的应用 |
| US12103924B2 (en) | 2020-06-01 | 2024-10-01 | Icahn School Of Medicine At Mount Sinai | Mitogen-activated protein kinase kinase (MEK) degradation compounds and methods of use |
| TW202328138A (zh) | 2021-09-17 | 2023-07-16 | 大陸商江蘇恒瑞醫藥股份有限公司 | 稠合二環類衍生物的可藥用鹽、晶型及其製備方法 |
| CN116514739B (zh) * | 2023-05-09 | 2025-07-22 | 天津绿菱气体股份有限公司 | 一种1,4-二甲基哌嗪及其制备方法 |
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