JP2010532386A5 - - Google Patents
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- JP2010532386A5 JP2010532386A5 JP2010515269A JP2010515269A JP2010532386A5 JP 2010532386 A5 JP2010532386 A5 JP 2010532386A5 JP 2010515269 A JP2010515269 A JP 2010515269A JP 2010515269 A JP2010515269 A JP 2010515269A JP 2010532386 A5 JP2010532386 A5 JP 2010532386A5
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- Prior art keywords
- compound according
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- Prior art date
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- 150000001875 compounds Chemical class 0.000 claims description 130
- -1 CH 2 F Chemical compound 0.000 claims description 65
- 125000000623 heterocyclic group Chemical group 0.000 claims description 22
- 125000004429 atom Chemical group 0.000 claims description 14
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 14
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 14
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 claims description 12
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims description 12
- 229910052799 carbon Inorganic materials 0.000 claims description 10
- 201000010099 disease Diseases 0.000 claims description 10
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 10
- 238000000034 method Methods 0.000 claims description 9
- UFWIBTONFRDIAS-UHFFFAOYSA-N Naphthalene Chemical compound C1=CC=CC2=CC=CC=C21 UFWIBTONFRDIAS-UHFFFAOYSA-N 0.000 claims description 8
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims description 8
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 8
- 125000000753 cycloalkyl group Chemical group 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
- 230000001404 mediated effect Effects 0.000 claims description 8
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 8
- 239000008194 pharmaceutical composition Substances 0.000 claims description 8
- 150000003839 salts Chemical class 0.000 claims description 8
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 6
- 241000124008 Mammalia Species 0.000 claims description 6
- 229910052736 halogen Inorganic materials 0.000 claims description 6
- 125000004043 oxo group Chemical group O=* 0.000 claims description 6
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 claims description 6
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 4
- ICSNLGPSRYBMBD-UHFFFAOYSA-N 2-aminopyridine Chemical compound NC1=CC=CC=N1 ICSNLGPSRYBMBD-UHFFFAOYSA-N 0.000 claims description 4
- 125000004800 4-bromophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Br 0.000 claims description 4
- 125000004801 4-cyanophenyl group Chemical group [H]C1=C([H])C(C#N)=C([H])C([H])=C1* 0.000 claims description 4
- 125000004199 4-trifluoromethylphenyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)C(F)(F)F 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
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 4
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims description 4
- 208000035475 disorder Diseases 0.000 claims description 4
- 239000003814 drug Substances 0.000 claims description 4
- 150000002367 halogens Chemical class 0.000 claims description 4
- 125000005842 heteroatom Chemical group 0.000 claims description 4
- 238000004519 manufacturing process Methods 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
- 125000004179 3-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(Cl)=C1[H] 0.000 claims description 2
- 125000004180 3-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(F)=C1[H] 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
- 208000024172 Cardiovascular disease Diseases 0.000 claims description 2
- WTKZEGDFNFYCGP-UHFFFAOYSA-N Pyrazole Chemical compound C=1C=NNC=1 WTKZEGDFNFYCGP-UHFFFAOYSA-N 0.000 claims description 2
- 125000000319 biphenyl-4-yl group Chemical group [H]C1=C([H])C([H])=C([H])C([H])=C1C1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 claims description 2
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims description 2
- 125000005843 halogen group Chemical group 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
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 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
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 claims description 2
- 125000003944 tolyl group Chemical group 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims 5
- 125000006661 (C4-C6) heterocyclic group Chemical group 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 description 12
- 0 C*C1(*)c2ncnc(N(CC3)C(*)CN3C(C(*)C3C(*)C*C(*)(*)*3)=O)c2C(*)(*)C1 Chemical compound C*C1(*)c2ncnc(N(CC3)C(*)CN3C(C(*)C3C(*)C*C(*)(*)*3)=O)c2C(*)(*)C1 0.000 description 4
- 125000006569 (C5-C6) heterocyclic group Chemical group 0.000 description 1
- 125000001412 tetrahydropyranyl group Chemical group 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US94813807P | 2007-07-05 | 2007-07-05 | |
| US60/948,138 | 2007-07-05 | ||
| US2008808P | 2008-01-09 | 2008-01-09 | |
| US61/020,088 | 2008-01-09 | ||
| PCT/US2008/069144 WO2009006567A2 (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 |
|---|---|---|---|
| JP2013207007A Division JP2014028842A (ja) | 2007-07-05 | 2013-10-02 | 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 |
|---|---|
| JP2010532386A JP2010532386A (ja) | 2010-10-07 |
| JP2010532386A5 true JP2010532386A5 (Direct) | 2012-07-26 |
| JP5628028B2 JP5628028B2 (ja) | 2014-11-19 |
Family
ID=40076864
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010515269A Active JP5628028B2 (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 |
| JP2013207007A Withdrawn JP2014028842A (ja) | 2007-07-05 | 2013-10-02 | 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 |
|---|---|---|---|
| JP2013207007A Withdrawn JP2014028842A (ja) | 2007-07-05 | 2013-10-02 | 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 (19)
| Country | Link |
|---|---|
| US (1) | US8618097B2 (Direct) |
| EP (1) | EP2170863B1 (Direct) |
| JP (2) | JP5628028B2 (Direct) |
| KR (2) | KR101650956B1 (Direct) |
| CN (2) | CN101801955B (Direct) |
| AR (1) | AR067413A1 (Direct) |
| AU (1) | AU2008272830B8 (Direct) |
| BR (1) | BRPI0813999A2 (Direct) |
| CA (1) | CA2692502C (Direct) |
| CO (1) | CO6251283A2 (Direct) |
| CR (1) | CR11229A (Direct) |
| EC (1) | ECSP109937A (Direct) |
| ES (1) | ES2551352T3 (Direct) |
| MA (1) | MA31679B1 (Direct) |
| NZ (1) | NZ582692A (Direct) |
| RU (1) | RU2486181C2 (Direct) |
| SG (1) | SG185274A1 (Direct) |
| TW (1) | TWI450720B (Direct) |
| WO (1) | WO2009006567A2 (Direct) |
Families Citing this family (33)
| Publication number | Priority date | Publication date | Assignee | Title |
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| WO2008036540A2 (en) | 2006-09-20 | 2008-03-27 | Boehringer Ingelheim International Gmbh | Rho kinase inhibitors |
| US8455513B2 (en) | 2007-01-10 | 2013-06-04 | Aerie Pharmaceuticals, Inc. | 6-aminoisoquinoline compounds |
| US9409886B2 (en) | 2007-07-05 | 2016-08-09 | Array Biopharma Inc. | Pyrimidyl cyclopentanes as AKT protein kinase inhibitors |
| US8846683B2 (en) | 2007-07-05 | 2014-09-30 | Array Biopharma, Inc. | Pyrimidyl cyclopentanes as Akt protein kinase inhibitors |
| EP2242755B1 (en) | 2008-01-08 | 2012-09-12 | 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 |
| MX2010007546A (es) | 2008-01-09 | 2010-09-30 | Array Biopharma Inc | Pirimidil ciclopentanos hidroxilados en forma de inhibidores de akt proteína quinasa. |
| CN102015708B (zh) | 2008-01-09 | 2014-03-26 | 阵列生物制药公司 | 作为akt蛋白激酶抑制剂的嘧啶基环戊烷 |
| KR101624753B1 (ko) | 2008-01-09 | 2016-05-26 | 어레이 바이오파마 인크. | Ａｋｔ 단백질 키나제 저해물질로서의 수산화된 피리미딜 시클로펜탄 |
| ES2392014T3 (es) | 2008-01-09 | 2012-12-03 | Array Biopharma, Inc. | Pirazolopiridinas como inhibidores de la cinasa |
| US8450344B2 (en) | 2008-07-25 | 2013-05-28 | Aerie Pharmaceuticals, Inc. | Beta- and gamma-amino-isoquinoline amide compounds and substituted benzamide compounds |
| CA2929545C (en) | 2009-05-01 | 2019-04-09 | Aerie Pharmaceuticals, Inc. | Dual mechanism inhibitors for the treatment of disease |
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| CA2850175C (en) | 2011-04-01 | 2021-04-13 | Genentech, Inc. | Biomarkers for predicting sensitivity to cancer treatments |
| SG11201407618VA (en) | 2012-05-17 | 2015-01-29 | Genentech Inc | Amorphous form of an akt inhibiting pyrimidinyl - cyclopentane compound, compositions and methods thereof |
| EA201590053A1 (ru) | 2012-06-20 | 2015-08-31 | Новартис Аг | Модуляторы пути системы комплемента и их применение |
| MX369175B (es) | 2013-02-25 | 2019-10-30 | Genentech Inc | Métodos para detectar mutantes de akt resistentes a fármacos. |
| FI3811943T3 (fi) | 2013-03-15 | 2023-04-14 | Aerie Pharmaceuticals Inc | Yhdiste käytettäväksi silmäsairauksien hoidossa |
| US9643927B1 (en) | 2015-11-17 | 2017-05-09 | Aerie Pharmaceuticals, Inc. | Process for the preparation of kinase inhibitors and intermediates thereof |
| JP6832946B2 (ja) | 2015-11-17 | 2021-02-24 | アエリエ ファーマシューティカルズ インコーポレイテッド | キナーゼ阻害剤およびその中間体の調製方法 |
| WO2017156350A1 (en) | 2016-03-09 | 2017-09-14 | K-Gen, Inc. | Methods of cancer treatment |
| BR112019003945A2 (pt) | 2016-08-31 | 2019-05-21 | Aerie Pharmaceuticals, Inc. | composições oftálmicas |
| WO2018081530A1 (en) | 2016-10-28 | 2018-05-03 | Icahn School Of Medicine At Mount Sinai | Compositions and methods for treating ezh2-mediated cancer |
| KR20190135027A (ko) | 2017-03-31 | 2019-12-05 | 에어리 파마슈티컬즈, 인코포레이티드 | 아릴 시클로프로필-아미노-이소퀴놀리닐 아미드 화합물 |
| CN112154146A (zh) * | 2018-03-06 | 2020-12-29 | 西奈山伊坎医学院 | 丝氨酸苏氨酸激酶(akt)降解/破坏化合物和使用方法 |
| BR112020020307A2 (pt) * | 2018-04-04 | 2021-01-12 | Arvinas Operations, Inc. | Moduladores de proteólise e métodos de uso associados |
| 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 |
| WO2020056345A1 (en) | 2018-09-14 | 2020-03-19 | Aerie Pharmaceuticals, Inc. | Aryl cyclopropyl-amino-isoquinolinyl amide compounds |
| US20220185796A1 (en) * | 2019-03-27 | 2022-06-16 | St. Jude Children's Research Hospital | Small molecule modulators of pank |
| EP3965824B1 (en) | 2019-05-06 | 2025-01-08 | Icahn School of Medicine at Mount Sinai | Heterobifunctional compounds as degraders of hpk1 |
| 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 |
| CN117677614A (zh) * | 2021-12-17 | 2024-03-08 | 中国医药研究开发中心有限公司 | 具有akt激酶抑制活性的杂环化合物及其制备方法和医药用途 |
| KR20250151412A (ko) | 2023-01-26 | 2025-10-21 | 아비나스 오퍼레이션스, 인코포레이티드 | 세레블론계 kras 분해 단백질 및 이와 관련된 용도 |
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