JP2015517532A5 - - Google Patents
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- Publication number
- JP2015517532A5 JP2015517532A5 JP2015512900A JP2015512900A JP2015517532A5 JP 2015517532 A5 JP2015517532 A5 JP 2015517532A5 JP 2015512900 A JP2015512900 A JP 2015512900A JP 2015512900 A JP2015512900 A JP 2015512900A JP 2015517532 A5 JP2015517532 A5 JP 2015517532A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- unsubstituted
- compound
- salt
- process according
- 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
Links
- 150000001875 compounds Chemical class 0.000 claims description 43
- 229910052739 hydrogen Inorganic materials 0.000 claims description 24
- 239000001257 hydrogen Substances 0.000 claims description 24
- 150000003839 salts Chemical class 0.000 claims description 24
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical group [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 15
- 125000000217 alkyl group Chemical group 0.000 claims description 15
- 125000000623 heterocyclic group Chemical group 0.000 claims description 15
- -1 Boc group Chemical group 0.000 claims description 14
- 125000002346 iodo group Chemical group I* 0.000 claims description 14
- 239000011777 magnesium Substances 0.000 claims description 10
- 125000001246 bromo group Chemical group Br* 0.000 claims description 9
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 9
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 9
- 125000006239 protecting group Chemical group 0.000 claims description 9
- 125000003342 alkenyl group Chemical group 0.000 claims description 8
- 125000000304 alkynyl group Chemical group 0.000 claims description 8
- 150000002431 hydrogen Chemical class 0.000 claims description 8
- 125000004429 atom Chemical group 0.000 claims description 7
- 239000003795 chemical substances by application Substances 0.000 claims description 6
- 229910052744 lithium Inorganic materials 0.000 claims description 6
- 229910052749 magnesium Inorganic materials 0.000 claims description 6
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims description 5
- LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 claims description 4
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 3
- WHXSMMKQMYFTQS-UHFFFAOYSA-N Lithium Chemical compound [Li] WHXSMMKQMYFTQS-UHFFFAOYSA-N 0.000 claims description 2
- FYYHWMGAXLPEAU-UHFFFAOYSA-N Magnesium Chemical compound [Mg] FYYHWMGAXLPEAU-UHFFFAOYSA-N 0.000 claims description 2
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 claims description 2
- 150000004791 alkyl magnesium halides Chemical group 0.000 claims description 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 2
- 125000001584 benzyloxycarbonyl group Chemical group C(=O)(OCC1=CC=CC=C1)* 0.000 claims description 2
- IUYHWZFSGMZEOG-UHFFFAOYSA-M magnesium;propane;chloride Chemical group [Mg+2].[Cl-].C[CH-]C IUYHWZFSGMZEOG-UHFFFAOYSA-M 0.000 claims description 2
- 125000005545 phthalimidyl group Chemical group 0.000 claims description 2
- 125000005931 tert-butyloxycarbonyl group Chemical group [H]C([H])([H])C(OC(*)=O)(C([H])([H])[H])C([H])([H])[H] 0.000 claims description 2
- 125000004044 trifluoroacetyl group Chemical group FC(C(=O)*)(F)F 0.000 claims description 2
- 125000002221 trityl group Chemical group [H]C1=C([H])C([H])=C([H])C([H])=C1C([*])(C1=C(C(=C(C(=C1[H])[H])[H])[H])[H])C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 claims description 2
- 125000005843 halogen group Chemical group 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 125000004043 oxo group Chemical group O=* 0.000 claims 1
- 0 C[C@](C*)c1c(N2CCN(*)CC2)ncnc1* Chemical compound C[C@](C*)c1c(N2CCN(*)CC2)ncnc1* 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261648473P | 2012-05-17 | 2012-05-17 | |
| US61/648,473 | 2012-05-17 | ||
| US201361785122P | 2013-03-14 | 2013-03-14 | |
| US61/785,122 | 2013-03-14 | ||
| PCT/US2013/041666 WO2013173768A1 (en) | 2012-05-17 | 2013-05-17 | Process for making hydroxylated cyclopentylpyrimidine compounds |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015517532A JP2015517532A (ja) | 2015-06-22 |
| JP2015517532A5 true JP2015517532A5 (enExample) | 2016-06-30 |
| JP6284928B2 JP6284928B2 (ja) | 2018-02-28 |
Family
ID=48485537
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015512900A Active JP6284928B2 (ja) | 2012-05-17 | 2013-05-17 | 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 |
Country Status (20)
| Country | Link |
|---|---|
| US (4) | US9416110B2 (enExample) |
| EP (1) | EP2861582B1 (enExample) |
| JP (1) | JP6284928B2 (enExample) |
| KR (1) | KR102067850B1 (enExample) |
| CN (1) | CN104470913B (enExample) |
| AU (1) | AU2013262505B2 (enExample) |
| BR (1) | BR112014028589B1 (enExample) |
| CA (1) | CA2873654C (enExample) |
| DK (1) | DK2861582T3 (enExample) |
| ES (1) | ES2582557T3 (enExample) |
| IL (1) | IL235715A (enExample) |
| MX (1) | MX353384B (enExample) |
| MY (1) | MY169028A (enExample) |
| NZ (1) | NZ702935A (enExample) |
| PL (1) | PL2861582T3 (enExample) |
| RU (1) | RU2643811C2 (enExample) |
| SG (1) | SG11201407616TA (enExample) |
| SI (1) | SI2861582T1 (enExample) |
| WO (1) | WO2013173768A1 (enExample) |
| ZA (1) | ZA201409261B (enExample) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK2861582T3 (en) | 2012-05-17 | 2016-08-22 | Array Biopharma Inc | A process for preparing hydroxylated compounds cyclopentylpyrimidin |
| SG11201407618VA (en) | 2012-05-17 | 2015-01-29 | Genentech Inc | Amorphous form of an akt inhibiting pyrimidinyl - cyclopentane compound, compositions and methods thereof |
| EP2850200A1 (en) | 2012-05-17 | 2015-03-25 | Genentech, Inc. | Process of making hydroxylated cyclopentapyrimidine compounds and salts thereof |
| ES2588878T3 (es) | 2012-05-17 | 2016-11-07 | Array Biopharma, Inc. | Proceso para preparar compuestos de ciclopentilpirimidina hidroxilada |
| CN105899492B (zh) | 2013-11-15 | 2021-08-24 | 豪夫迈·罗氏有限公司 | 用于制备嘧啶基环戊烷化合物的方法 |
| CA2962901A1 (en) * | 2014-09-26 | 2016-03-31 | F.Hoffmann-La Roche Ag | Processes for preparing (cyclopentyl[d]pyrimidin-4-yl)piperazine compounds |
| KR102766096B1 (ko) | 2016-08-10 | 2025-02-12 | 에프. 호프만-라 로슈 아게 | Akt 단백질 키나아제 저해제를 포함하는 약학 조성물 |
| CN115916758A (zh) | 2020-06-16 | 2023-04-04 | 豪夫迈·罗氏有限公司 | 用于制备羟基化环戊基嘧啶化合物的方法 |
| KR102689151B1 (ko) * | 2021-09-06 | 2024-07-29 | 연세대학교 산학협력단 | Akt 신호경로 억제제를 유효성분으로 포함하는 아토피피부염의 예방 또는 치료용 조성물 |
Family Cites Families (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH09506369A (ja) | 1993-12-12 | 1997-06-24 | アグロジーン・リミテッド | 菌類感染から植物を保護するための新規方法 |
| JP2001524079A (ja) | 1997-04-07 | 2001-11-27 | メルク エンド カンパニー インコーポレーテッド | ガンの治療方法 |
| US6201023B1 (en) | 1997-06-10 | 2001-03-13 | Agrogene Ltd. | Methods and compositions to protect crops against plant parasitic nematodes |
| EP0982300A3 (en) | 1998-07-29 | 2000-03-08 | Societe Civile Bioprojet | Non-imidazole alkylamines as histamine H3 - receptor ligands and their therapeutic applications |
| AU3386600A (en) | 1999-03-03 | 2000-09-21 | Merck & Co., Inc. | Inhibitors of prenyl-protein transferase |
| ES2239596T3 (es) * | 1999-06-03 | 2005-10-01 | Teikoku Hormone Mfg. Co., Ltd. | Compuestos de pirazol sustituidos. |
| WO2001022963A1 (en) | 1999-09-27 | 2001-04-05 | Merck & Co., Inc. | Method of preventing osteoporosis |
| JP4550811B2 (ja) | 2003-06-09 | 2010-09-22 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | パピローマウイルスのインヒビター |
| US8927546B2 (en) | 2006-02-28 | 2015-01-06 | Dart Neuroscience (Cayman) Ltd. | Therapeutic piperazines |
| US8063050B2 (en) * | 2006-07-06 | 2011-11-22 | Array Biopharma Inc. | Hydroxylated and methoxylated pyrimidyl cyclopentanes as AKT protein kinase inhibitors |
| UA95641C2 (xx) | 2006-07-06 | 2011-08-25 | Эррей Биофарма Инк. | Гідроксильовані піримідильні циклопентани як інгібітори акт протеїнкінази$гидроксилированные пиримидильные циклопентаны как ингибиторы акт протеинкиназы |
| EP2209775A1 (en) | 2007-10-09 | 2010-07-28 | UCB Pharma, S.A. | Heterobicyclic compounds as histamine h4-receptor antagonists |
| JP5734956B2 (ja) | 2009-04-15 | 2015-06-17 | アッヴィ・インコーポレイテッド | 抗ウィルス化合物 |
| KR101398268B1 (ko) * | 2009-10-23 | 2014-05-23 | 일라이 릴리 앤드 캄파니 | Ａｋｔ 억제제 |
| US9050334B2 (en) | 2010-07-16 | 2015-06-09 | Innov88 Llc | MIF inhibitors and their uses |
| WO2012177925A1 (en) | 2011-06-21 | 2012-12-27 | The Board Institute, Inc. | Akt inhibitors for treating cancer expressing a magi3 - akt3 fusion gene |
| EP2850200A1 (en) | 2012-05-17 | 2015-03-25 | Genentech, Inc. | Process of making hydroxylated cyclopentapyrimidine compounds and salts thereof |
| SG11201407618VA (en) | 2012-05-17 | 2015-01-29 | Genentech Inc | Amorphous form of an akt inhibiting pyrimidinyl - cyclopentane compound, compositions and methods thereof |
| KR102074535B1 (ko) | 2012-05-17 | 2020-02-06 | 제넨테크, 인크. | 아미노산 화합물의 제조 방법 |
| DK2861582T3 (en) | 2012-05-17 | 2016-08-22 | Array Biopharma Inc | A process for preparing hydroxylated compounds cyclopentylpyrimidin |
| ES2588878T3 (es) | 2012-05-17 | 2016-11-07 | Array Biopharma, Inc. | Proceso para preparar compuestos de ciclopentilpirimidina hidroxilada |
| US20140121193A1 (en) | 2012-11-01 | 2014-05-01 | Robert S. Katz | Methods for treating fibromyalgia |
| CA2901577A1 (en) | 2013-02-18 | 2014-08-21 | The Scripps Research Institute | Modulators of vasopressin receptors with therapeutic potential |
| US10131637B2 (en) | 2013-03-15 | 2018-11-20 | Shifa Biomedical Corporation | Anti-PCSK9 compounds and methods for the treatment and/or prevention of cardiovascular diseases |
-
2013
- 2013-05-17 DK DK13725042.9T patent/DK2861582T3/en active
- 2013-05-17 US US14/401,087 patent/US9416110B2/en active Active
- 2013-05-17 EP EP13725042.9A patent/EP2861582B1/en active Active
- 2013-05-17 WO PCT/US2013/041666 patent/WO2013173768A1/en not_active Ceased
- 2013-05-17 MY MYPI2014703415A patent/MY169028A/en unknown
- 2013-05-17 JP JP2015512900A patent/JP6284928B2/ja active Active
- 2013-05-17 SG SG11201407616TA patent/SG11201407616TA/en unknown
- 2013-05-17 AU AU2013262505A patent/AU2013262505B2/en active Active
- 2013-05-17 ES ES13725042.9T patent/ES2582557T3/es active Active
- 2013-05-17 CA CA2873654A patent/CA2873654C/en active Active
- 2013-05-17 SI SI201330261A patent/SI2861582T1/sl unknown
- 2013-05-17 CN CN201380038057.4A patent/CN104470913B/zh active Active
- 2013-05-17 PL PL13725042.9T patent/PL2861582T3/pl unknown
- 2013-05-17 KR KR1020147035427A patent/KR102067850B1/ko active Active
- 2013-05-17 MX MX2014013862A patent/MX353384B/es active IP Right Grant
- 2013-05-17 BR BR112014028589-6A patent/BR112014028589B1/pt active IP Right Grant
- 2013-05-17 NZ NZ702935A patent/NZ702935A/en not_active IP Right Cessation
- 2013-05-17 RU RU2014151050A patent/RU2643811C2/ru active
-
2014
- 2014-11-13 IL IL235715A patent/IL235715A/en active IP Right Grant
- 2014-12-15 ZA ZA2014/09261A patent/ZA201409261B/en unknown
-
2016
- 2016-07-07 US US15/204,715 patent/US9676730B2/en active Active
-
2017
- 2017-05-11 US US15/593,064 patent/US9790190B2/en active Active
- 2017-10-12 US US15/782,620 patent/US20180258054A1/en not_active Abandoned