CN102574852B - Akt抑制剂 - Google Patents

Akt抑制剂 Download PDF

Info

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

Links

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 (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=)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US12617784B2 (en) 2019-01-29 2026-05-05 Nanjing Chia Tai Tianqing Pharmaceutical Co., Ltd. AKT inhibitor

Families Citing this family (18)

* Cited by examiner, † Cited by third party
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 (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

Family Cites Families (17)

* Cited by examiner, † Cited by third party
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
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

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US12617784B2 (en) 2019-01-29 2026-05-05 Nanjing Chia Tai Tianqing Pharmaceutical Co., Ltd. AKT inhibitor

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
AU2010310786B2 (en) 2014-03-27
EA201270590A1 (ru) 2012-09-28
EA020151B1 (ru) 2014-09-30

Similar Documents

Publication Publication Date Title
CN102574852B (zh) Akt抑制剂
JP7833597B2 (ja) Ｃｄｋ２阻害剤としての二環式アミン
CN114728938B (zh) 作为prmt5抑制剂的四氢异喹啉螺环化合物
CN107428760A (zh) (s)‑n‑(5‑((r)‑2‑(2,5‑二氟苯基)‑吡咯烷‑1‑基)‑吡唑并[1,5‑a]嘧啶‑3‑基)‑3‑羟基吡咯烷‑1‑甲酰胺硫酸氢盐的晶型
JP2013536253A5 (https=)
EP4346815A1 (en) Heterocyclic compounds and methods of use
AU2023312000A1 (en) Cyclic compounds and methods of using same
EP4472974A2 (en) Heterocyclic compounds and methods of use
WO2021113492A1 (en) Cyclic compounds and methods of using same
EP4308573B1 (en) Cyclic compounds and methods of using same
CN117715642A (zh) 杂环化合物和使用方法
HK40127987A (en) Cyclic compounds and methods of using same
EP4539832A2 (en) Phenyl amide compounds and methods of use
WO2025059027A1 (en) Cyclopenta[e]pyrazolo[1,5-a]pyrimidine derivatives as malt1 inhibitors
HK40099028A (zh) 氧氮杂䓬化合物及其在癌症治疗中的用途
CN116490507A (zh) 用于治疗癌症的杂环包缩合cdc7激酶抑制剂
CN117120447A (zh) 环状化合物和其使用方法

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
C14 Grant of patent or utility model
GR01 Patent grant
CF01 Termination of patent right due to non-payment of annual fee

Granted publication date: 20140625

Termination date: 20151020

EXPY Termination of patent right or utility model