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 (enExample
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)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Oncology (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (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 (enExample) 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 (enExample)
EP (1) EP1948188A4 (enExample)
JP (1) JP2009516653A (enExample)
KR (1) KR20080067646A (enExample)
AP (1) AP2008004442A0 (enExample)
AR (1) AR056786A1 (enExample)
AU (1) AU2006315805A1 (enExample)
BR (1) BRPI0618309A2 (enExample)
CA (1) CA2629429A1 (enExample)
EA (1) EA200801301A1 (enExample)
EC (1) ECSP088425A (enExample)
IL (1) IL190968A0 (enExample)
MA (1) MA29935B1 (enExample)
NO (1) NO20082414L (enExample)
TW (1) TW200736260A (enExample)
WO (1) WO2007058850A2 (enExample)

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)

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EP1948185A4 (en) * 2005-11-10 2010-04-21 Glaxosmithkline Llc INHIBITORS OF AKT ACTIVITY
EP3358354B1 (en) 2008-01-18 2020-07-15 President and Fellows of Harvard College Methods of detecting signatures of disease or conditions in bodily fluids
UA103319C2 (en) 2008-05-06 2013-10-10 Глаксосмитклайн Ллк Thiazole- and oxazole-benzene sulfonamide compounds
US20110086834A1 (en) * 2008-06-26 2011-04-14 Amgen Inc. Alkynyl alcohols as kinase inhibitors
JP5702293B2 (ja) 2008-11-10 2015-04-15 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化合物
BRPI0924084B1 (pt) 2008-12-19 2021-12-21 Vertex Pharmaceuticals Incorporated Derivados de pirazina e composição farmacêutica que os compreende
WO2011143422A1 (en) 2010-05-12 2011-11-17 Vertex Pharmaceuticals Incorporated 2 -aminopyridine derivatives useful as inhibitors of atr kinase
JP2013526538A (ja) 2010-05-12 2013-06-24 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 Ａｔｒキナーゼ阻害剤として有用な化合物
US9062008B2 (en) 2010-05-12 2015-06-23 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
EP2569287B1 (en) 2010-05-12 2014-07-09 Vertex Pharmaceuticals Inc. Compounds useful as inhibitors of atr kinase
AU2011253025A1 (en) 2010-05-12 2012-11-29 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
WO2011163527A1 (en) 2010-06-23 2011-12-29 Vertex Pharmaceuticals Incorporated Pyrrolo- pyrazine derivatives useful as inhibitors of atr kinase
SG10201505724SA (en) * 2010-07-23 2015-09-29 Harvard College Methods of detecting diseases or conditions using phagocytic cells
US20130203624A1 (en) 2010-07-23 2013-08-08 President And Fellows Of Harvard College Methods of Detecting Prenatal or Pregnancy-Related Diseases or Conditions
CA2806293A1 (en) 2010-07-23 2012-01-26 President And Fellows Of Harvard College Methods of detecting autoimmune or immune-related diseases or conditions
KR20130133051A (ko) 2011-03-16 2013-12-05 에프. 호프만-라 로슈 아게 6,5-헤테로사이클릭 프로파길릭 알콜 화합물 및 이의 용도
WO2012138938A1 (en) 2011-04-05 2012-10-11 Vertex Pharmaceuticals Incorporated Aminopyrazine compounds useful as inhibitors of tra kinase
JP2014517079A (ja) 2011-06-22 2014-07-17 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 Ａｔｒキナーゼ阻害剤として有用な化合物
EP2723745A1 (en) 2011-06-22 2014-04-30 Vertex Pharmaceuticals Inc. Compounds useful as inhibitors of atr kinase
JP2014522818A (ja) 2011-06-22 2014-09-08 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 Ａｔｒキナーゼ阻害剤として有用な化合物
WO2013049719A1 (en) 2011-09-30 2013-04-04 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
MX2014003796A (es) 2011-09-30 2015-01-16 Vertex Pharma Compuestos utiles como inhibidores de la cinasa ataxia telangiectasia mutada y rad3 relacionados (atr).
SG10201606774UA (en) 2011-09-30 2016-10-28 Vertex Pharma Processes for making compounds useful as inhibitors of atr kinase
WO2013049720A1 (en) 2011-09-30 2013-04-04 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
IN2014CN02501A (enExample) 2011-09-30 2015-06-26 Vertex Pharma
WO2013071093A1 (en) 2011-11-09 2013-05-16 Vertex Pharmaceuticals Incorporated Pyrazine compounds useful as inhibitors of atr kinase
EP2776422A1 (en) 2011-11-09 2014-09-17 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
US8841449B2 (en) 2011-11-09 2014-09-23 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
EP2776421A1 (en) 2011-11-09 2014-09-17 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
EP2776429A1 (en) 2011-11-09 2014-09-17 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
US20140044802A1 (en) 2012-04-05 2014-02-13 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase and combination therapies thereof
DK2904406T3 (en) 2012-10-04 2018-06-18 Vertex Pharma METHOD OF DETERMINING THE ATR INHIBITION, INCREASED DNA DAMAGE
US8912198B2 (en) 2012-10-16 2014-12-16 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
SMT202000713T1 (it) 2012-12-07 2021-03-15 Vertex Pharma Pirazolo [1,5-a] pirimidine utili come inibitori dell'atr chinasi per il trattamento di malattie del cancro
EP4202441A3 (en) 2013-03-09 2023-07-26 Immunis.AI, Inc. Gene expression profile in macrophages for the diagnosis of cancer
JP2016512815A (ja) 2013-03-15 2016-05-09 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縮合ピラゾロピリミジン誘導体
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
CA2928568A1 (en) 2013-07-26 2015-01-29 Update Pharma Inc. Combinatorial methods to improve the therapeutic benefit of bisantrene
HUE046727T2 (hu) 2013-12-06 2020-03-30 Vertex Pharma Az ATR-kináz inhibitoraként használható vegyület, 2-amino-6-fluoro-N-[5-fluoro-piridin-3-IL]-pirazolo-[1,5-A]-pirimidin-3-karboxamid, ennek elõállítása, különbözõ szilárd formái és ezek radioaktív nyomjelzett származékai
CN107074863B (zh) 2014-06-05 2019-12-03 沃泰克斯药物股份有限公司 Atr激酶抑制剂的制备方法及其不同的固体形式
PL3157566T3 (pl) 2014-06-17 2019-10-31 Vertex Pharma Metoda leczenia nowotworu przy użyciu kombinacji inhibitorów chk1 i atr
MX371151B (es) 2014-10-23 2020-01-20 Janssen Pharmaceutica Nv NUEVOS DERIVADOS DE TIENOPIRIMIDINA EN CALIDAD DE INHIBIDORES DE LA CINASA INDUCTORA DE NF-kB (NIK).
BR112017007704B1 (pt) 2014-10-23 2023-04-11 Janssen Pharmaceutica N.V Derivados de pirazolopirimidina como inibidores de nik, seu uso e composição farmacêutica que os compreende
US9981962B2 (en) 2014-10-23 2018-05-29 Janssen Pharmaceutica Nv Pyrazole derivatives as NIK inhibitors
ES2718557T3 (es) 2014-10-23 2019-07-02 Janssen Pharmaceutica Nv Nuevos compuestos como inhibidores de nik
KR102678021B1 (ko) 2015-09-30 2024-06-26 버텍스 파마슈티칼스 인코포레이티드 Dna 손상제와 병용되는, atr 저해제를 포함하는 암 치료용 약제학적 조성물
WO2020078865A1 (en) 2018-10-16 2020-04-23 F. Hoffmann-La Roche Ag Use of akt inhibitors in ophthalmology
PE20211655A1 (es) 2018-10-31 2021-08-24 Gilead Sciences Inc Compuestos de 6-azabencimidazol sustituidos como inhibidores de hpk1
WO2020092528A1 (en) 2018-10-31 2020-05-07 Gilead Sciences, Inc. Substituted 6-azabenzimidazole compounds having hpk1 inhibitory activity
TWI826690B (zh) 2019-05-23 2023-12-21 美商基利科學股份有限公司 經取代之烯吲哚酮化物及其用途
CN119278041A (zh) 2022-03-31 2025-01-07 阿斯利康(瑞典)有限公司 用于治疗癌症的与akt抑制剂组合的表皮生长因子受体（egfr）酪氨酸激酶抑制剂
CN120051280A (zh) 2022-10-17 2025-05-27 阿斯利康(瑞典)有限公司 用于治疗癌症的serd的组合
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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
AR056786A1 (es) 2007-10-24
AP2008004442A0 (en) 2008-04-30
MA29935B1 (fr) 2008-11-03
AU2006315805A1 (en) 2007-05-24
KR20080067646A (ko) 2008-07-21
EP1948188A2 (en) 2008-07-30
WO2007058850A3 (en) 2009-04-30
BRPI0618309A2 (pt) 2011-08-23
TW200736260A (en) 2007-10-01
ECSP088425A (es) 2008-06-30
US20100056523A1 (en) 2010-03-04
CA2629429A1 (en) 2007-05-24
EP1948188A4 (en) 2011-02-16
NO20082414L (no) 2008-08-05
EA200801301A1 (ru) 2009-02-27
WO2007058850A2 (en) 2007-05-24
IL190968A0 (en) 2009-02-11

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