AU2010310786B2 - AKT inhibitors - Google Patents
AKT inhibitors Download PDFInfo
- Publication number
- AU2010310786B2 AU2010310786B2 AU2010310786A AU2010310786A AU2010310786B2 AU 2010310786 B2 AU2010310786 B2 AU 2010310786B2 AU 2010310786 A AU2010310786 A AU 2010310786A AU 2010310786 A AU2010310786 A AU 2010310786A AU 2010310786 B2 AU2010310786 B2 AU 2010310786B2
- Authority
- AU
- Australia
- Prior art keywords
- imidazol
- ethyl
- tert
- butyl
- piperidine
- 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.)
- Ceased
Links
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- 229940124597 therapeutic agent Drugs 0.000 claims description 11
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- ZWCMRPLHSMWBIQ-UHFFFAOYSA-N tert-butyl 4-[4-(oxan-4-yl)-1-[2-(oxan-2-yloxy)ethyl]imidazol-2-yl]piperidine-1-carboxylate Chemical compound C1CN(C(=O)OC(C)(C)C)CCC1C1=NC(C2CCOCC2)=CN1CCOC1OCCCC1 ZWCMRPLHSMWBIQ-UHFFFAOYSA-N 0.000 description 1
- KDPJVSDTIUBBQI-UHFFFAOYSA-N tert-butyl 4-[4-cyclopropyl-1-[2-(oxan-2-yloxy)ethyl]imidazol-2-yl]piperidine-1-carboxylate Chemical compound C1CN(C(=O)OC(C)(C)C)CCC1C1=NC(C2CC2)=CN1CCOC1OCCCC1 KDPJVSDTIUBBQI-UHFFFAOYSA-N 0.000 description 1
- BFNIIQIAMUFQTM-UHFFFAOYSA-N tert-butyl 4-[4-ethenyl-1-(2-pyrrolidin-1-ylethyl)imidazol-2-yl]piperidine-1-carboxylate Chemical compound C1CN(C(=O)OC(C)(C)C)CCC1C1=NC(C=C)=CN1CCN1CCCC1 BFNIIQIAMUFQTM-UHFFFAOYSA-N 0.000 description 1
- QHSHGQVUKATCLP-UHFFFAOYSA-N tert-butyl 4-[4-ethyl-1-(2-hydroxyethyl)imidazol-2-yl]piperidine-1-carboxylate Chemical compound CCC1=CN(CCO)C(C2CCN(CC2)C(=O)OC(C)(C)C)=N1 QHSHGQVUKATCLP-UHFFFAOYSA-N 0.000 description 1
- TUPFTCWZDWDOFF-UHFFFAOYSA-N tert-butyl 4-[4-ethyl-1-[2-(oxan-2-yloxy)ethyl]imidazol-2-yl]piperidine-1-carboxylate Chemical compound C1CN(C(=O)OC(C)(C)C)CCC1C1=NC(CC)=CN1CCOC1CCCCO1 TUPFTCWZDWDOFF-UHFFFAOYSA-N 0.000 description 1
- GXQWBHYONHVBKF-UHFFFAOYSA-N tert-butyl 4-[5-(2-methylpropyl)-1h-imidazol-2-yl]piperidine-1-carboxylate Chemical compound CC(C)CC1=CNC(C2CCN(CC2)C(=O)OC(C)(C)C)=N1 GXQWBHYONHVBKF-UHFFFAOYSA-N 0.000 description 1
- YBRBMKDOPFTVDT-UHFFFAOYSA-N tert-butylamine Chemical compound CC(C)(C)N YBRBMKDOPFTVDT-UHFFFAOYSA-N 0.000 description 1
- 238000012360 testing method Methods 0.000 description 1
- 210000001519 tissue Anatomy 0.000 description 1
- 229940100411 torisel Drugs 0.000 description 1
- ZFDIRQKJPRINOQ-UHFFFAOYSA-N transbutenic acid ethyl ester Natural products CCOC(=O)C=CC ZFDIRQKJPRINOQ-UHFFFAOYSA-N 0.000 description 1
- 230000001131 transforming effect Effects 0.000 description 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 description 1
- BWHDROKFUHTORW-UHFFFAOYSA-O tritert-butylphosphanium Chemical compound CC(C)(C)[PH+](C(C)(C)C)C(C)(C)C BWHDROKFUHTORW-UHFFFAOYSA-O 0.000 description 1
- 238000003828 vacuum filtration Methods 0.000 description 1
- 239000003039 volatile agent Substances 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US25430809P | 2009-10-23 | 2009-10-23 | |
| US61/254,308 | 2009-10-23 | ||
| PCT/US2010/053295 WO2011050016A1 (en) | 2009-10-23 | 2010-10-20 | Akt inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| AU2010310786A1 AU2010310786A1 (en) | 2012-04-19 |
| AU2010310786B2 true AU2010310786B2 (en) | 2014-03-27 |
Family
ID=43467018
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2010310786A Ceased AU2010310786B2 (en) | 2009-10-23 | 2010-10-20 | AKT inhibitors |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US8436002B2 (https=) |
| EP (1) | EP2491032B1 (https=) |
| JP (1) | JP5581390B2 (https=) |
| KR (1) | KR101398268B1 (https=) |
| CN (1) | CN102574852B (https=) |
| AU (1) | AU2010310786B2 (https=) |
| BR (1) | BR112012011328A2 (https=) |
| CA (1) | CA2778291C (https=) |
| EA (1) | EA020151B1 (https=) |
| ES (1) | ES2465094T3 (https=) |
| MX (1) | MX2012004780A (https=) |
| WO (1) | WO2011050016A1 (https=) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HRP20180948T1 (hr) | 2012-05-17 | 2018-08-10 | Genentech, Inc. | Postupak za proizvodnju aminokiselinskih spojeva |
| EP2850200A1 (en) | 2012-05-17 | 2015-03-25 | Genentech, Inc. | Process of making hydroxylated cyclopentapyrimidine compounds and salts thereof |
| US9416110B2 (en) | 2012-05-17 | 2016-08-16 | Array Biopharma Inc. | Process for making hydroxylated cyclopentylpyrimidine compounds |
| ES2588878T3 (es) | 2012-05-17 | 2016-11-07 | Array Biopharma, Inc. | Proceso para preparar compuestos de ciclopentilpirimidina hidroxilada |
| KR102678074B1 (ko) | 2012-05-17 | 2024-06-26 | 제넨테크, 인크. | 무정형 형태의 akt 저해성 피리미디닐 - 사이클로펜탄 화합물, 조성물 및 이들의 방법 |
| EP2920154B1 (en) * | 2012-11-16 | 2017-10-11 | Merck Patent GmbH | Novel imidazol-piperidinyl derivatives as modulators of kinase activity |
| AR095202A1 (es) * | 2013-03-11 | 2015-09-30 | Merck Patent Gmbh | Heterociclos como moduladores de la actividad quinasa |
| CN112472699A (zh) | 2013-07-26 | 2021-03-12 | 种族肿瘤学公司 | 改善比生群及衍生物的治疗益处的组合方法 |
| AU2014318614B2 (en) | 2013-09-12 | 2021-01-07 | Dana-Farber Cancer Institute Inc. | Methods for evaluating and treating Waldenstrom's macroglobulinemia |
| GB201401198D0 (en) * | 2014-01-24 | 2014-03-12 | Bial Portela & Ca Sa | Process for the syntheis of substituted urea compounds |
| EP3476392A1 (en) | 2014-02-28 | 2019-05-01 | Merck Sharp & Dohme Corp. | Method for treating cancer |
| PT3459953T (pt) * | 2016-05-20 | 2021-07-29 | Taiho Pharmaceutical Co Ltd | Novo derivado de 5h-pirrolo[2,3-d]pirimidin-6(7h)-ona |
| AU2020214258B2 (en) * | 2019-01-29 | 2025-08-28 | Nanjing Chia Tai Tianqing Pharmaceutical Co., Ltd. | AKT inhibitor |
| JP2023525757A (ja) * | 2020-05-08 | 2023-06-19 | ジョージアミューン・インコーポレイテッド | Ａｋｔ３モジュレーター |
| CN115485276B (zh) * | 2020-05-15 | 2024-05-31 | 南京正大天晴制药有限公司 | 氘代akt激酶抑制剂 |
| US20230321108A1 (en) * | 2020-07-22 | 2023-10-12 | Nanjing Chia Tai Tianqing Pharmaceutical Co., Ltd. | Unit dosage composition of akt inhibitor |
| WO2022017448A1 (zh) * | 2020-07-22 | 2022-01-27 | 南京正大天晴制药有限公司 | 一种二氢吡啶并[2,3-d]嘧啶酮衍生物的盐及晶型 |
| US20230286979A1 (en) * | 2020-07-22 | 2023-09-14 | Nanjing Chia Tai Tianqing Pharmaceutical Co., Ltd. | Salt of dihydropyrido[2,3-d]pyrimidinone derivative, preparation method therefor, and use thereof |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2008075109A1 (en) * | 2006-12-21 | 2008-06-26 | Astex Therapeutics Limited | Substituted piperidines having protein kinase inhibiting activity |
Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU4128089A (en) | 1988-09-15 | 1990-03-22 | Rorer International (Overseas) Inc. | Monoclonal antibodies specific to human epidermal growth factor receptor and therapeutic methods employing same |
| GB9300059D0 (en) | 1992-01-20 | 1993-03-03 | Zeneca Ltd | Quinazoline derivatives |
| GB9221220D0 (en) | 1992-10-09 | 1992-11-25 | Sandoz Ag | Organic componds |
| US5362718A (en) | 1994-04-18 | 1994-11-08 | American Home Products Corporation | Rapamycin hydroxyesters |
| NL1004346C2 (nl) | 1996-10-23 | 1998-04-24 | Dsm Nv | Werkwijze voor het scheiden van een mengsel van enantiomeren in een geschikt oplosmiddel. |
| PT1478648E (pt) | 2002-02-01 | 2014-07-15 | Ariad Pharma Inc | Compostos contendo fósforo e suas utilizações |
| US7563748B2 (en) | 2003-06-23 | 2009-07-21 | Cognis Ip Management Gmbh | Alcohol alkoxylate carriers for pesticide active ingredients |
| WO2005117909A2 (en) | 2004-04-23 | 2005-12-15 | Exelixis, Inc. | Kinase modulators and methods of use |
| RU2346996C2 (ru) | 2004-06-29 | 2009-02-20 | ЮРОПИЭН НИКЕЛЬ ПиЭлСи | Усовершенствованное выщелачивание основных металлов |
| MY179032A (en) | 2004-10-25 | 2020-10-26 | Cancer Research Tech Ltd | Ortho-condensed pyridine and pyrimidine derivatives (e.g.purines) as protein kinase inhibitors |
| US7767687B2 (en) | 2004-12-13 | 2010-08-03 | Biogen Idec Ma Inc. | Pyrido pyrimidinones, dihydro pyrimido pyrimidinones and pteridinones useful as RAF kinase inhibitors |
| JP5274842B2 (ja) * | 2004-12-28 | 2013-08-28 | エグゼリクシス， インコーポレイテッド | 免疫疾患、炎症疾患および増殖疾患の処置のためのセリン−スレオニンキナーゼモジュレーター（ｐ７０Ｓ６Ｋ、Ａｋｔ−１およびＡｋｔ−２）としての［１Ｈ−ピペラゾ［３，４−ｄ］ピリミジン−４−イル］−ピペラジンまたは［１Ｈ−ピペラゾ［３，４−ｄ］ピリミジン−４−イル］−ピペラジン化合物 |
| US7930013B2 (en) | 2005-06-29 | 2011-04-19 | Compumedics Limited | Sensor assembly with conductive bridge |
| DK3421471T3 (da) | 2006-04-25 | 2021-06-14 | Astex Therapeutics Ltd | Purin- og deazapurinderivater som farmaceutiske forbindelser |
| JP2009534456A (ja) * | 2006-04-25 | 2009-09-24 | アステックス、セラピューティックス、リミテッド | 医薬化合物 |
| TW200801513A (en) | 2006-06-29 | 2008-01-01 | Fermiscan Australia Pty Ltd | Improved process |
| UA99284C2 (ru) * | 2007-05-11 | 2012-08-10 | Елі Ліллі Енд Компані | ИНГИБИТОРЫ р70 S6-КИНАЗЫ |
| AR074072A1 (es) * | 2008-11-11 | 2010-12-22 | Lilly Co Eli | Compuesto de imidazol -piperidin -pirrol-pirimidin-6-ona, composicion farmaceutica que lo comprende y su uso para preparar un medicamento util para tratar el glioblastoma multiforme |
-
2010
- 2010-10-20 EA EA201270590A patent/EA020151B1/ru not_active IP Right Cessation
- 2010-10-20 BR BR112012011328A patent/BR112012011328A2/pt not_active IP Right Cessation
- 2010-10-20 KR KR1020127010282A patent/KR101398268B1/ko not_active Expired - Fee Related
- 2010-10-20 AU AU2010310786A patent/AU2010310786B2/en not_active Ceased
- 2010-10-20 MX MX2012004780A patent/MX2012004780A/es active IP Right Grant
- 2010-10-20 US US13/391,895 patent/US8436002B2/en not_active Expired - Fee Related
- 2010-10-20 JP JP2012535319A patent/JP5581390B2/ja not_active Expired - Fee Related
- 2010-10-20 CN CN201080046941.9A patent/CN102574852B/zh not_active Expired - Fee Related
- 2010-10-20 CA CA2778291A patent/CA2778291C/en not_active Expired - Fee Related
- 2010-10-20 EP EP10774072.2A patent/EP2491032B1/en not_active Not-in-force
- 2010-10-20 ES ES10774072.2T patent/ES2465094T3/es active Active
- 2010-10-20 WO PCT/US2010/053295 patent/WO2011050016A1/en not_active Ceased
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2008075109A1 (en) * | 2006-12-21 | 2008-06-26 | Astex Therapeutics Limited | Substituted piperidines having protein kinase inhibiting activity |
Also Published As
| Publication number | Publication date |
|---|---|
| EP2491032B1 (en) | 2014-04-16 |
| MX2012004780A (es) | 2012-08-23 |
| WO2011050016A1 (en) | 2011-04-28 |
| ES2465094T3 (es) | 2014-06-05 |
| AU2010310786A1 (en) | 2012-04-19 |
| JP2013508382A (ja) | 2013-03-07 |
| CN102574852A (zh) | 2012-07-11 |
| EP2491032A1 (en) | 2012-08-29 |
| JP5581390B2 (ja) | 2014-08-27 |
| BR112012011328A2 (pt) | 2016-11-22 |
| KR20120068941A (ko) | 2012-06-27 |
| US20120149684A1 (en) | 2012-06-14 |
| CA2778291C (en) | 2014-02-11 |
| US8436002B2 (en) | 2013-05-07 |
| KR101398268B1 (ko) | 2014-05-23 |
| CA2778291A1 (en) | 2011-04-28 |
| EA201270590A1 (ru) | 2012-09-28 |
| EA020151B1 (ru) | 2014-09-30 |
| CN102574852B (zh) | 2014-06-25 |
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| FGA | Letters patent sealed or granted (standard patent) | ||
| MK14 | Patent ceased section 143(a) (annual fees not paid) or expired |