KR101398268B1 - Ａｋｔ 억제제 - Google Patents

Ａｋｔ 억제제 Download PDF

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Publication number
KR101398268B1
KR101398268B1 KR1020127010282A KR20127010282A KR101398268B1 KR 101398268 B1 KR101398268 B1 KR 101398268B1 KR 1020127010282 A KR1020127010282 A KR 1020127010282A KR 20127010282 A KR20127010282 A KR 20127010282A KR 101398268 B1 KR101398268 B1 KR 101398268B1
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KR
South Korea
Prior art keywords
compound
tert
added
butyl
ethyl
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Expired - Fee Related
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KR1020127010282A
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English (en)
Korean (ko)
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KR20120068941A (ko
Inventor
더글라스 웨이드 바이트
티모시 폴 버크홀더
조슈아 리안 클레이튼
마리진 에겐
케네쓰 제임스 주니어 헨리
데이드레 미셸 존스
사라바난 파르타사라티
후아싱 페이
마크 에드워드 렘팔라
제이슨 스콧 소이어
Original Assignee
일라이 릴리 앤드 캄파니
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Publication of KR20120068941A publication Critical patent/KR20120068941A/ko
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Publication of KR101398268B1 publication Critical patent/KR101398268B1/ko
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    • 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

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  • 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)
KR1020127010282A 2009-10-23 2010-10-20 Ａｋｔ 억제제 Expired - Fee Related KR101398268B1 (ko)

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
KR20120068941A KR20120068941A (ko) 2012-06-27
KR101398268B1 true KR101398268B1 (ko) 2014-05-23

Family

ID=43467018

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020127010282A Expired - Fee Related KR101398268B1 (ko) 2009-10-23 2010-10-20 Ａｋｔ 억제제

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=)

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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 (2)

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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
WO2008140947A1 (en) 2007-05-11 2008-11-20 Eli Lilly And Company P70 s6 kinase inhibitors

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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
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

Patent Citations (2)

* Cited by examiner, † Cited by third party
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
WO2008140947A1 (en) 2007-05-11 2008-11-20 Eli Lilly And Company P70 s6 kinase inhibitors

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
CA2778291A1 (en) 2011-04-28
AU2010310786B2 (en) 2014-03-27
EA201270590A1 (ru) 2012-09-28
EA020151B1 (ru) 2014-09-30
CN102574852B (zh) 2014-06-25

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