JP2015518837A5 - - Google Patents
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- Publication number
- JP2015518837A5 JP2015518837A5 JP2015512890A JP2015512890A JP2015518837A5 JP 2015518837 A5 JP2015518837 A5 JP 2015518837A5 JP 2015512890 A JP2015512890 A JP 2015512890A JP 2015512890 A JP2015512890 A JP 2015512890A JP 2015518837 A5 JP2015518837 A5 JP 2015518837A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- salt
- formula
- process according
- forming
- 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 34
- 238000000034 method Methods 0.000 claims description 31
- 150000003839 salts Chemical class 0.000 claims description 29
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical group [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 8
- 239000003054 catalyst Substances 0.000 claims description 8
- 125000000217 alkyl group Chemical group 0.000 claims description 5
- 230000006315 carbonylation Effects 0.000 claims description 4
- 238000005810 carbonylation reaction Methods 0.000 claims description 4
- 229910052739 hydrogen Inorganic materials 0.000 claims description 4
- 239000001257 hydrogen Substances 0.000 claims description 4
- 238000006114 decarboxylation reaction Methods 0.000 claims description 3
- 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 3
- -1 Boc group Chemical group 0.000 claims description 2
- UGFAIRIUMAVXCW-UHFFFAOYSA-N Carbon monoxide Chemical compound [O+]#[C-] UGFAIRIUMAVXCW-UHFFFAOYSA-N 0.000 claims description 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 2
- PNKUSGQVOMIXLU-UHFFFAOYSA-N Formamidine Chemical compound NC=N PNKUSGQVOMIXLU-UHFFFAOYSA-N 0.000 claims description 2
- 102000004882 Lipase Human genes 0.000 claims description 2
- 108090001060 Lipase Proteins 0.000 claims description 2
- 239000004367 Lipase Substances 0.000 claims description 2
- KJTLSVCANCCWHF-UHFFFAOYSA-N Ruthenium Chemical compound [Ru] KJTLSVCANCCWHF-UHFFFAOYSA-N 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
- 229910002091 carbon monoxide Inorganic materials 0.000 claims description 2
- 229910052736 halogen Inorganic materials 0.000 claims description 2
- 150000002367 halogens Chemical class 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
- 235000019421 lipase Nutrition 0.000 claims description 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 2
- 229910052763 palladium Inorganic materials 0.000 claims description 2
- LPNYRYFBWFDTMA-UHFFFAOYSA-N potassium tert-butoxide Chemical compound [K+].CC(C)(C)[O-] LPNYRYFBWFDTMA-UHFFFAOYSA-N 0.000 claims description 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 2
- 125000006239 protecting group Chemical group 0.000 claims description 2
- 229910052707 ruthenium Inorganic materials 0.000 claims description 2
- 0 C[C@](C*)c(c(Cl)ncn1)c1Cl Chemical compound C[C@](C*)c(c(Cl)ncn1)c1Cl 0.000 description 1
- 230000000911 decarboxylating effect Effects 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261648421P | 2012-05-17 | 2012-05-17 | |
| US61/648,421 | 2012-05-17 | ||
| US201361785281P | 2013-03-14 | 2013-03-14 | |
| US61/785,281 | 2013-03-14 | ||
| PCT/US2013/041624 WO2013173736A1 (en) | 2012-05-17 | 2013-05-17 | Process for making hydroxylated cyclopentylpyrimidine compounds |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015518837A JP2015518837A (ja) | 2015-07-06 |
| JP2015518837A5 true JP2015518837A5 (enExample) | 2016-07-07 |
| JP6214636B2 JP6214636B2 (ja) | 2017-10-18 |
Family
ID=48534507
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015512890A Active JP6214636B2 (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 (18)
| Country | Link |
|---|---|
| US (1) | US9309204B2 (enExample) |
| EP (1) | EP2861583B1 (enExample) |
| JP (1) | JP6214636B2 (enExample) |
| KR (1) | KR20150020211A (enExample) |
| CN (1) | CN104487430B (enExample) |
| AU (1) | AU2013262568B2 (enExample) |
| BR (1) | BR112014028570A2 (enExample) |
| CA (1) | CA2873653A1 (enExample) |
| DK (1) | DK2861583T3 (enExample) |
| ES (1) | ES2588878T3 (enExample) |
| IL (1) | IL235714A0 (enExample) |
| MA (1) | MA37649B1 (enExample) |
| MX (1) | MX2014013865A (enExample) |
| PL (1) | PL2861583T3 (enExample) |
| RU (1) | RU2014151017A (enExample) |
| SG (1) | SG11201407613RA (enExample) |
| SI (1) | SI2861583T1 (enExample) |
| WO (1) | WO2013173736A1 (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 |
| KR102074535B1 (ko) | 2012-05-17 | 2020-02-06 | 제넨테크, 인크. | 아미노산 화합물의 제조 방법 |
| 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 |
| 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 |
| AU2014356984B2 (en) * | 2013-11-27 | 2018-01-04 | Sunshine Lake Pharma Co., Ltd. | Processes for preparing dihydropyrimidine derivatives and intermediates thereof |
| CA2962901A1 (en) * | 2014-09-26 | 2016-03-31 | F.Hoffmann-La Roche Ag | Processes for preparing (cyclopentyl[d]pyrimidin-4-yl)piperazine compounds |
| 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 (27)
| 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 |
| AU2004293026B2 (en) | 2003-11-21 | 2012-01-19 | Array Biopharma Inc. | AKT protein kinase inhibitors |
| 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 |
| JP5157576B2 (ja) | 2007-05-14 | 2013-03-06 | 住友化学株式会社 | 光学活性2−アルキル−1,1,3−トリアルコキシカルボニルプロパンの製造方法 |
| KR20150091196A (ko) * | 2007-07-05 | 2015-08-07 | 어레이 바이오파마 인크. | Akt 단백질 키나제 억제제로서의 피리미딜 시클로펜탄 |
| EP2209775A1 (en) | 2007-10-09 | 2010-07-28 | UCB Pharma, S.A. | Heterobicyclic compounds as histamine h4-receptor antagonists |
| CA2711699A1 (en) * | 2008-01-09 | 2009-07-16 | Array Biopharma Inc. | Hydroxylated pyrimidyl cyclopentanes as akt protein kinase inhibitors |
| JP5551707B2 (ja) * | 2008-10-15 | 2014-07-16 | アムジエン・インコーポレーテツド | スピロ環gpr40調節因子 |
| 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 |
| KR102074535B1 (ko) | 2012-05-17 | 2020-02-06 | 제넨테크, 인크. | 아미노산 화합물의 제조 방법 |
| EP2850200A1 (en) | 2012-05-17 | 2015-03-25 | Genentech, Inc. | Process of making hydroxylated cyclopentapyrimidine compounds and salts thereof |
| DK2861582T3 (en) | 2012-05-17 | 2016-08-22 | Array Biopharma Inc | A process for preparing hydroxylated compounds cyclopentylpyrimidin |
| 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 ES ES13725533.7T patent/ES2588878T3/es active Active
- 2013-05-17 US US14/401,091 patent/US9309204B2/en active Active
- 2013-05-17 RU RU2014151017A patent/RU2014151017A/ru not_active Application Discontinuation
- 2013-05-17 CA CA2873653A patent/CA2873653A1/en not_active Abandoned
- 2013-05-17 CN CN201380037994.8A patent/CN104487430B/zh active Active
- 2013-05-17 DK DK13725533.7T patent/DK2861583T3/en active
- 2013-05-17 EP EP13725533.7A patent/EP2861583B1/en active Active
- 2013-05-17 AU AU2013262568A patent/AU2013262568B2/en not_active Ceased
- 2013-05-17 BR BR112014028570A patent/BR112014028570A2/pt not_active IP Right Cessation
- 2013-05-17 KR KR20147035262A patent/KR20150020211A/ko not_active Withdrawn
- 2013-05-17 WO PCT/US2013/041624 patent/WO2013173736A1/en not_active Ceased
- 2013-05-17 SG SG11201407613RA patent/SG11201407613RA/en unknown
- 2013-05-17 PL PL13725533.7T patent/PL2861583T3/pl unknown
- 2013-05-17 MX MX2014013865A patent/MX2014013865A/es unknown
- 2013-05-17 SI SI201330302A patent/SI2861583T1/sl unknown
- 2013-05-17 MA MA37649A patent/MA37649B1/fr unknown
- 2013-05-17 JP JP2015512890A patent/JP6214636B2/ja active Active
-
2014
- 2014-11-13 IL IL235714A patent/IL235714A0/en unknown
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