CN102574852B - Akt抑制剂 - Google Patents

Akt抑制剂 Download PDF

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Publication number
CN102574852B
CN102574852B CN201080046941.9A CN201080046941A CN102574852B CN 102574852 B CN102574852 B CN 102574852B CN 201080046941 A CN201080046941 A CN 201080046941A CN 102574852 B CN102574852 B CN 102574852B
Authority
CN
China
Prior art keywords
compound
imidazol
ethyl
tert
methyl
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.)
Expired - Fee Related
Application number
CN201080046941.9A
Other languages
English (en)
Chinese (zh)
Other versions
CN102574852A (zh
Inventor
D·W·贝特
T·P·伯克霍德尔
J·R·克莱顿
M·埃根
K·J·J·亨利
D·M·琼斯
S·帕塔萨拉蒂
裴华兴
M·E·莱帕拉
J·S·索耶
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Eli Lilly and Co
Original Assignee
Eli Lilly and Co
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Eli Lilly and Co filed Critical Eli Lilly and Co
Publication of CN102574852A publication Critical patent/CN102574852A/zh
Application granted granted Critical
Publication of CN102574852B publication Critical patent/CN102574852B/zh
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

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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)
CN201080046941.9A 2009-10-23 2010-10-20 Akt抑制剂 Expired - Fee Related CN102574852B (zh)

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
CN102574852A CN102574852A (zh) 2012-07-11
CN102574852B true CN102574852B (zh) 2014-06-25

Family

ID=43467018

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201080046941.9A Expired - Fee Related CN102574852B (zh) 2009-10-23 2010-10-20 Akt抑制剂

Country Status (12)

Country Link
US (1) US8436002B2 (enExample)
EP (1) EP2491032B1 (enExample)
JP (1) JP5581390B2 (enExample)
KR (1) KR101398268B1 (enExample)
CN (1) CN102574852B (enExample)
AU (1) AU2010310786B2 (enExample)
BR (1) BR112012011328A2 (enExample)
CA (1) CA2778291C (enExample)
EA (1) EA020151B1 (enExample)
ES (1) ES2465094T3 (enExample)
MX (1) MX2012004780A (enExample)
WO (1) WO2011050016A1 (enExample)

Families Citing this family (17)

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ES2588878T3 (es) 2012-05-17 2016-11-07 Array Biopharma, Inc. Proceso para preparar compuestos de ciclopentilpirimidina hidroxilada
HRP20180948T1 (hr) 2012-05-17 2018-08-10 Genentech, Inc. Postupak za proizvodnju aminokiselinskih spojeva
NZ702935A (en) 2012-05-17 2017-02-24 Genentech Inc Process for making hydroxylated cyclopentylpyrimidine compounds
EP3719014A1 (en) 2012-05-17 2020-10-07 Genentech, Inc. Solid forms of an akt inhibiting pyrimidinyl-cyclopentane compound, compositions and methods thereof
CA2873661C (en) 2012-05-17 2020-07-21 Genentech, Inc. Process of making hydroxylated cyclopentapyrimidine compounds and salts thereof
ES2656096T3 (es) * 2012-11-16 2018-02-23 Merck Patent Gmbh Nuevos derivados de imidazol-piperidinilo como moduladores de la actividad de quinasa
AU2014228385B2 (en) * 2013-03-11 2018-08-09 Merck Patent Gmbh 6-[4-(1-H-imidazol-2-yl]piperidin-1 -yl]pyrimidin-4-amine derivatives as modulators of kinase activity
AU2014293013A1 (en) 2013-07-26 2016-03-17 Race Oncology Ltd. Combinatorial methods to improve the therapeutic benefit of bisantrene
US10526660B2 (en) 2013-09-12 2020-01-07 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
EP3110509B1 (en) 2014-02-28 2020-08-19 Merck Sharp & Dohme Corp. Treating cancer with a combination comprising dinaciclib
MA45048A (fr) * 2016-05-20 2019-03-27 Taiho Pharmaceutical Co Ltd Nouveau dérivé de 5h-pyrrolo[2,3-d]pyrimidin-6(7h)-one
CN113272304B (zh) * 2019-01-29 2024-03-29 南京正大天晴制药有限公司 Akt抑制剂
WO2021228223A1 (zh) * 2020-05-15 2021-11-18 南京正大天晴制药有限公司 氘代akt激酶抑制剂
CA3186568A1 (en) * 2020-07-22 2022-01-27 Changyou MA Salt of dihydropyrido[2,3-d]pyrimidinone derivative, preparation method therefor, and use thereof
US20230271958A1 (en) * 2020-07-22 2023-08-31 Nanjing Chia Tai Tianqing Pharmaceutical Co., Ltd. SALT AND CRYSTAL FORM OF DIHYDROPYRIDO[2,3-d]PYRIMIDINE DERIVATE
US20230321108A1 (en) * 2020-07-22 2023-10-12 Nanjing Chia Tai Tianqing Pharmaceutical Co., Ltd. Unit dosage composition of akt inhibitor

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

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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
AU661533B2 (en) 1992-01-20 1995-07-27 Astrazeneca Ab 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.
WO2003064383A2 (en) 2002-02-01 2003-08-07 Ariad Gene Therapeutics, Inc. Phosphorus-containing compounds & uses thereof
US7563748B2 (en) 2003-06-23 2009-07-21 Cognis Ip Management Gmbh Alcohol alkoxylate carriers for pesticide active ingredients
US8076338B2 (en) 2004-04-23 2011-12-13 Exelixis, Inc. Kinase modulators and methods of use
WO2006000020A1 (en) 2004-06-29 2006-01-05 European Nickel Plc Improved leaching of base metals
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
JP5111113B2 (ja) * 2004-12-13 2012-12-26 サネシス ファーマシューティカルズ， インコーポレイテッド Ｒａｆキナーゼ阻害剤として有用なピリドピリミジノン、ジヒドロピリミドピリミジノンおよびプテリジノン
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
ES2360232T3 (es) 2005-06-29 2011-06-02 Compumedics Limited Conjunto sensor con puente conductor.
EP3719018B1 (en) 2006-04-25 2025-08-27 Astex Therapeutics Ltd Purine and deazapurine derivatives as pharmaceutical compounds
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
AU2010310786B2 (en) 2014-03-27
JP5581390B2 (ja) 2014-08-27
ES2465094T3 (es) 2014-06-05
AU2010310786A1 (en) 2012-04-19
KR101398268B1 (ko) 2014-05-23
MX2012004780A (es) 2012-08-23
WO2011050016A1 (en) 2011-04-28
US20120149684A1 (en) 2012-06-14
CA2778291C (en) 2014-02-11
CN102574852A (zh) 2012-07-11
BR112012011328A2 (pt) 2016-11-22
EA201270590A1 (ru) 2012-09-28
EP2491032B1 (en) 2014-04-16
US8436002B2 (en) 2013-05-07
KR20120068941A (ko) 2012-06-27
CA2778291A1 (en) 2011-04-28
JP2013508382A (ja) 2013-03-07
EP2491032A1 (en) 2012-08-29
EA020151B1 (ru) 2014-09-30

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Granted publication date: 20140625

Termination date: 20151020

EXPY Termination of patent right or utility model