JP2009516653A - Ａｋｔ活性の阻害剤 - Google Patents

Ａｋｔ活性の阻害剤 Download PDF

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Publication number
JP2009516653A
JP2009516653A JP2008540168A JP2008540168A JP2009516653A JP 2009516653 A JP2009516653 A JP 2009516653A JP 2008540168 A JP2008540168 A JP 2008540168A JP 2008540168 A JP2008540168 A JP 2008540168A JP 2009516653 A JP2009516653 A JP 2009516653A
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JP
Japan
Prior art keywords
cancer
methyl
pharmaceutically acceptable
compound
ethyl
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.)
Pending
Application number
JP2008540168A
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English (en)
Japanese (ja)
Other versions
JP2009516653A5 (https=
Inventor
ディルク・アー・ヘールディング
タミー・ジェイ・クラーク
ジャック・デイル・レーバー
イゴール・サフォノフ
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.)
SmithKline Beecham Corp
Original Assignee
SmithKline Beecham Corp
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 SmithKline Beecham Corp filed Critical SmithKline Beecham Corp
Publication of JP2009516653A publication Critical patent/JP2009516653A/ja
Publication of JP2009516653A5 publication Critical patent/JP2009516653A5/ja
Pending legal-status Critical Current

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Classifications

    • 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
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541—Non-condensed thiazines containing further heterocyclic rings
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4245—Oxadiazoles
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
    • A61K31/5517—1,4-Benzodiazepines, e.g. diazepam or clozapine condensed with five-membered rings having nitrogen as a ring hetero atom, e.g. imidazobenzodiazepines, triazolam
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
JP2008540168A 2005-11-10 2006-11-09 Ａｋｔ活性の阻害剤 Pending JP2009516653A (ja)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US73595505P 2005-11-10 2005-11-10
US77228906P 2006-02-10 2006-02-10
US82692806P 2006-09-26 2006-09-26
PCT/US2006/043513 WO2007058850A2 (en) 2005-11-10 2006-11-09 Inhibitors of akt activity

Publications (2)

Publication Number Publication Date
JP2009516653A true JP2009516653A (ja) 2009-04-23
JP2009516653A5 JP2009516653A5 (https=) 2009-12-17

Family

ID=38049129

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2008540168A Pending JP2009516653A (ja) 2005-11-10 2006-11-09 Ａｋｔ活性の阻害剤

Country Status (16)

Country Link
US (1) US20100056523A1 (https=)
EP (1) EP1948188A4 (https=)
JP (1) JP2009516653A (https=)
KR (1) KR20080067646A (https=)
AP (1) AP2008004442A0 (https=)
AR (1) AR056786A1 (https=)
AU (1) AU2006315805A1 (https=)
BR (1) BRPI0618309A2 (https=)
CA (1) CA2629429A1 (https=)
EA (1) EA200801301A1 (https=)
EC (1) ECSP088425A (https=)
IL (1) IL190968A0 (https=)
MA (1) MA29935B1 (https=)
NO (1) NO20082414L (https=)
TW (1) TW200736260A (https=)
WO (1) WO2007058850A2 (https=)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2011521214A (ja) * 2008-05-16 2011-07-21 セルゾーム アーゲー Ｐａｒｐ相互作用分子の同定およびｐａｒｐタンパク質の精製のための方法
JP2016531858A (ja) * 2013-09-26 2016-10-13 ヤンセン ファーマシューティカ エヌ．ベー． 新規な、ＮＩＫ阻害剤としての３−（１Ｈ−ピラゾール−４−イル）−１Ｈ−ピロロ［２，３−ｃ］ピリジン誘導体
JP2016531868A (ja) * 2013-09-26 2016-10-13 ヤンセン ファーマシューティカ エヌ．ベー． 新規な、ＮＩＫ阻害剤としての１−（４−ピリミジニル）−１Ｈ−ピロロ［３，２−ｃ］ピリジン誘導体

Families Citing this family (55)

* Cited by examiner, † Cited by third party
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EP1948185A4 (en) * 2005-11-10 2010-04-21 Glaxosmithkline Llc INHIBITORS OF AKT ACTIVITY
MX340916B (es) 2008-01-18 2016-07-29 President And Fellows Of Harvard College * Metodos para detectar señales de identificacion de enfermedad o condiciones en fluidos corporales.
UA103319C2 (en) 2008-05-06 2013-10-10 Глаксосмитклайн Ллк Thiazole- and oxazole-benzene sulfonamide compounds
JP2011525915A (ja) * 2008-06-26 2011-09-29 アムジエン・インコーポレーテツド キナーゼ阻害薬としてのアルキニルアルコール類
CA2743134A1 (en) 2008-11-10 2010-05-14 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
ES2921576T3 (es) 2008-12-19 2022-08-29 Vertex Pharma Compuestos útiles como inhibidores de la quinasa ATR
CA2798760A1 (en) 2010-05-12 2011-11-17 Vertex Pharmaceuticals Incorporated 2-aminopyridine derivatives useful as inhibitors of atr kinase
US9334244B2 (en) 2010-05-12 2016-05-10 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
US8962631B2 (en) 2010-05-12 2015-02-24 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
NZ603477A (en) 2010-05-12 2014-09-26 Vertex Pharma Compounds useful as inhibitors of atr kinase
US9062008B2 (en) 2010-05-12 2015-06-23 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
EP2568984A1 (en) 2010-05-12 2013-03-20 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
MX2013000103A (es) 2010-06-23 2013-06-13 Vertex Pharma Derivados de pirrolo-pirazina utiles como inhibidores de cinasa art.
US20130203624A1 (en) 2010-07-23 2013-08-08 President And Fellows Of Harvard College Methods of Detecting Prenatal or Pregnancy-Related Diseases or Conditions
AU2011280997A1 (en) 2010-07-23 2013-02-28 President And Fellows Of Harvard College Methods of detecting autoimmune or immune-related diseases or conditions
TW201209171A (en) * 2010-07-23 2012-03-01 Harvard College Methods of detecting diseases or conditions using phagocytic cells
MX2013010513A (es) 2011-03-16 2013-10-07 Hoffmann La Roche Compuestos de alcohol 6,5-heterociclil-propargilico y usos de los mismos.
MX2013011450A (es) 2011-04-05 2014-02-03 Vertex Pharma Compuestos de aminopirazina utiles como inhibidores de la cinasa ataxia telangiectasia mutada y rad3 relacionados (atr).
EP2723747A1 (en) 2011-06-22 2014-04-30 Vertex Pharmaceuticals Inc. Compounds useful as inhibitors of atr kinase
US9309250B2 (en) 2011-06-22 2016-04-12 Vertex Pharmaceuticals Incorporated Substituted pyrrolo[2,3-b]pyrazines as ATR kinase inhibitors
US8822469B2 (en) 2011-06-22 2014-09-02 Vertex Pharmaceuticals Incorporated Pyrrolo[2,3-B]pyrazines useful as inhibitors of ATR kinase
WO2013049720A1 (en) 2011-09-30 2013-04-04 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
WO2013049722A1 (en) 2011-09-30 2013-04-04 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
US8765751B2 (en) 2011-09-30 2014-07-01 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
CN108685922A (zh) 2011-09-30 2018-10-23 沃泰克斯药物股份有限公司 用atr抑制剂治疗胰腺癌和非小细胞肺癌
CN106496173A (zh) 2011-09-30 2017-03-15 沃泰克斯药物股份有限公司 用于制备可用作atr激酶抑制剂的化合物的方法
US8846918B2 (en) 2011-11-09 2014-09-30 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
US8841337B2 (en) 2011-11-09 2014-09-23 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
US8841450B2 (en) 2011-11-09 2014-09-23 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
US8846917B2 (en) 2011-11-09 2014-09-30 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
JP2015502925A (ja) 2011-11-09 2015-01-29 バーテックス ファーマシューティカルズ インコーポレイテッドＶｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ Ａｔｒキナーゼの阻害剤として有用なピラジン化合物
CN108478577A (zh) 2012-04-05 2018-09-04 沃泰克斯药物股份有限公司 可用作atr激酶抑制剂的化合物及其组合疗法
DK2904406T3 (en) 2012-10-04 2018-06-18 Vertex Pharma METHOD OF DETERMINING THE ATR INHIBITION, INCREASED DNA DAMAGE
EP2909202A1 (en) 2012-10-16 2015-08-26 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
SI2941432T1 (en) 2012-12-07 2018-07-31 Vertex Pharmaceuticals Incorporated 2-AMINO-6-FLUORO-N- (5-FLUORO-4- (4- (4- (OXETHAN-3-YL) PIPERAZIN-1-CARBONYL) PIPERIDIN-1-YLIPRIDIN-3-YL) 1,5 ALFA) PYRIMIDINE-3-CARBOXAMIDE AS ATR KINAZE INHIBITOR
NZ771629A (en) 2013-03-09 2022-12-23 Harry Stylli Methods of detecting cancer
WO2014143240A1 (en) 2013-03-15 2014-09-18 Vertex Pharmaceuticals Incorporated Fused pyrazolopyrimidine derivatives useful as inhibitors of atr kinase
TWI663166B (zh) 2013-04-24 2019-06-21 健生藥品公司 新化合物
ES2909438T3 (es) * 2013-06-26 2022-05-06 Helmholtz Zentrum Muenchen Deutsches Forschungszentrum Gesundheit & Umwelt Gmbh Enantiómero (S) de mepacina como inhibidor de paracaspasa (MALT1) para tratar cáncer
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
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MX373102B (es) 2014-06-05 2020-04-17 Vertex Pharma Derivados radiomarcados de un compuesto de 2-amino-6-fluoro-n-[5-fluoro-piridin-3-il]-pirazolo[1,5-a]pirimidin-3-carboxamida útil como inhibidor de ataxia telangiectasia mutada y rad3 relacionado (atr) cinasa, preparación de tal compuesto y diferentes formas sólidas del mismo.
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KR102523405B1 (ko) 2014-10-23 2023-04-18 얀센 파마슈티카 엔.브이. Ｎｉｋ 억제제로서의 신규 피라졸로피리미딘 유도체
EA033238B1 (ru) 2014-10-23 2019-09-30 Янссен Фармацевтика Нв Новые производные тиенопиримидина в качестве ингибиторов nik
EP3209654B1 (en) 2014-10-23 2018-10-03 Janssen Pharmaceutica N.V. New pyrazole derivatives as nik inhibitors
AU2016331955B2 (en) 2015-09-30 2022-07-21 Vertex Pharmaceuticals Incorporated Method for treating cancer using a combination of DNA damaging agents and ATR inhibitors
CN112888440A (zh) 2018-10-16 2021-06-01 豪夫迈·罗氏有限公司 Akt抑制剂在眼科中的用途
WO2020092528A1 (en) 2018-10-31 2020-05-07 Gilead Sciences, Inc. Substituted 6-azabenzimidazole compounds having hpk1 inhibitory activity
US11203591B2 (en) 2018-10-31 2021-12-21 Gilead Sciences, Inc. Substituted 6-azabenzimidazole compounds
EP3972695A1 (en) 2019-05-23 2022-03-30 Gilead Sciences, Inc. Substituted exo-methylene-oxindoles which are hpk1/map4k1 inhibitors
JP2025510910A (ja) 2022-03-31 2025-04-15 アストラゼネカ・アクチエボラーグ 癌の処置のための、ａｋｔ阻害剤との組み合わせにおける上皮成長因子受容体（ｅｇｆｒ）チロシンキナーゼ阻害剤
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WO2024100236A1 (en) 2022-11-11 2024-05-16 Astrazeneca Ab Combination therapies for the treatment of cancer

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005011700A1 (en) * 2003-07-29 2005-02-10 Smithkline Beecham Corporation INHIBITORS OF Akt ACTIVITY

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005011700A1 (en) * 2003-07-29 2005-02-10 Smithkline Beecham Corporation INHIBITORS OF Akt ACTIVITY

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2011521214A (ja) * 2008-05-16 2011-07-21 セルゾーム アーゲー Ｐａｒｐ相互作用分子の同定およびｐａｒｐタンパク質の精製のための方法
JP2016531858A (ja) * 2013-09-26 2016-10-13 ヤンセン ファーマシューティカ エヌ．ベー． 新規な、ＮＩＫ阻害剤としての３−（１Ｈ−ピラゾール−４−イル）−１Ｈ−ピロロ［２，３−ｃ］ピリジン誘導体
JP2016531868A (ja) * 2013-09-26 2016-10-13 ヤンセン ファーマシューティカ エヌ．ベー． 新規な、ＮＩＫ阻害剤としての１−（４−ピリミジニル）−１Ｈ−ピロロ［３，２−ｃ］ピリジン誘導体

Also Published As

Publication number Publication date
KR20080067646A (ko) 2008-07-21
CA2629429A1 (en) 2007-05-24
AU2006315805A1 (en) 2007-05-24
IL190968A0 (en) 2009-02-11
MA29935B1 (fr) 2008-11-03
WO2007058850A3 (en) 2009-04-30
EP1948188A4 (en) 2011-02-16
WO2007058850A2 (en) 2007-05-24
TW200736260A (en) 2007-10-01
US20100056523A1 (en) 2010-03-04
AP2008004442A0 (en) 2008-04-30
EP1948188A2 (en) 2008-07-30
EA200801301A1 (ru) 2009-02-27
BRPI0618309A2 (pt) 2011-08-23
ECSP088425A (es) 2008-06-30
NO20082414L (no) 2008-08-05
AR056786A1 (es) 2007-10-24

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