JP2009516653A - Ａｋｔ活性の阻害剤 - Google Patents

Ａｋｔ活性の阻害剤 Download PDF

Info

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
Authority
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
Other languages
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

Links

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)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Oncology (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 (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
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
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

Families Citing this family (55)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20090227616A1 (en) * 2005-11-10 2009-09-10 Smithkline Beecham Corporation, A Corporation Inhibitors of akt activity
DK2240781T3 (en) 2008-01-18 2018-03-26 Harvard College METHODS FOR DETECTING DISEASE OR STATE SIGNATURES IN BODY FLUIDS
UA103319C2 (en) 2008-05-06 2013-10-10 Глаксосмитклайн Ллк Thiazole- and oxazole-benzene sulfonamide compounds
AU2009263037B2 (en) * 2008-06-26 2011-10-06 Amgen Inc. Alkynyl alcohols as kinase inhibitors
KR20170015566A (ko) 2008-11-10 2017-02-08 버텍스 파마슈티칼스 인코포레이티드 Ａｔｒ 키나제의 억제제로서 유용한 화합물
ES2663222T3 (es) 2008-12-19 2018-04-11 Vertex Pharmaceuticals Incorporated Derivados de pirazina útiles como inhibidores de la quinasa ATR
JP2013526540A (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
JP5856151B2 (ja) 2010-05-12 2016-02-09 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キナーゼ阻害剤として有用な２−アミノピリジン誘導体
JP2013529200A (ja) 2010-05-12 2013-07-18 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
US8969356B2 (en) 2010-05-12 2015-03-03 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
JP2013526539A (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ピラジン
US9630956B2 (en) 2010-05-12 2017-04-25 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
CA2803802A1 (en) 2010-06-23 2011-12-29 Vertex Pharmaceuticals Incorporated Pyrrolo- pyrazine derivatives useful as inhibitors of atr kinase
EP2596134B1 (en) * 2010-07-23 2020-04-08 President and Fellows of Harvard College Methods of detecting diseases or conditions using phagocytic cells
AU2011280997A1 (en) 2010-07-23 2013-02-28 President And Fellows Of Harvard College Methods of detecting autoimmune or immune-related diseases or conditions
CA2806304A1 (en) 2010-07-23 2012-01-26 President And Fellows Of Harvard College Methods of detecting prenatal or pregnancy-related diseases or conditions
MX2013010513A (es) * 2011-03-16 2013-10-07 Hoffmann La Roche Compuestos de alcohol 6,5-heterociclil-propargilico y usos de los mismos.
JP2014510151A (ja) 2011-04-05 2014-04-24 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（ｔｒａｋｉｎａｓｅ）阻害剤として有用なアミノピラジン化合物
EP2723745A1 (en) 2011-06-22 2014-04-30 Vertex Pharmaceuticals Inc. Compounds useful as inhibitors of atr kinase
WO2012178125A1 (en) 2011-06-22 2012-12-27 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
WO2012178124A1 (en) 2011-06-22 2012-12-27 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
US8853217B2 (en) 2011-09-30 2014-10-07 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
KR20140084112A (ko) 2011-09-30 2014-07-04 버텍스 파마슈티칼스 인코포레이티드 Ａｔｒ 키나제의 억제제로서 유용한 화합물
WO2013049859A1 (en) 2011-09-30 2013-04-04 Vertex Pharmaceuticals Incorporated Treating pancreatic cancer and non-small cell lung cancer with atr inhibitors
WO2013049719A1 (en) 2011-09-30 2013-04-04 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
SG10201606774UA (en) 2011-09-30 2016-10-28 Vertex Pharma Processes for making compounds useful as inhibitors of atr kinase
WO2013071088A1 (en) 2011-11-09 2013-05-16 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
US8841337B2 (en) 2011-11-09 2014-09-23 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
WO2013071085A1 (en) 2011-11-09 2013-05-16 Vertex Pharmaceuticals Incorporated Pyrazine compounds useful as inhibitors of atr kinase
WO2013071094A1 (en) 2011-11-09 2013-05-16 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
CA2869309C (en) 2012-04-05 2021-02-09 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase and combination therapies thereof
US8999632B2 (en) 2012-10-04 2015-04-07 Vertex Pharmaceuticals Incorporated Method for measuring ATR inhibition mediated increases in DNA damage
US8912198B2 (en) 2012-10-16 2014-12-16 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
EP2965077B1 (en) 2013-03-09 2022-07-13 Harry Stylli Methods of detecting 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
CN105764501A (zh) 2013-07-26 2016-07-13 现代化制药公司 改善比生群治疗效益的组合物
DK3077397T3 (da) 2013-12-06 2019-12-16 Vertex Pharma 2-amino-6-fluor-n-[5-fluor-pyridin-3-yl]pyrazolo[1,5-a]pyrimidin-3-carboxamidforbindelse anvendelig som atr-kinase-inhibitor, dens fremstilling, forskellige faste former og radiomarkerede derivater deraf
PL3152212T3 (pl) 2014-06-05 2020-06-15 Vertex Pharmaceuticals Inc. Radioznakowane pochodne związku 2-amino-6-fluoro-n-[5-fluoro-piridyn-3-ylo]-pirazolo[1,5-a]pirymidino-3-karboksamidu przydatne jako inhibitor kinazy atr, wytwarzanie tego związku i jego różnych postaci stałych
LT3157566T (lt) 2014-06-17 2019-08-12 Vertex Pharmaceuticals Incorporated Vėžio gydymo būdas, panaudojant chk1 ir atr inhibitorių derinį
AU2015334917B2 (en) 2014-10-23 2019-08-29 Janssen Pharmaceutica Nv New compounds as NIK inhibitors
JP6616412B2 (ja) 2014-10-23 2019-12-04 ヤンセン ファーマシューティカ エヌ．ベー． Ｎｉｋ阻害剤としての新規のピラゾロピリミジン誘導体
BR112017008039B1 (pt) 2014-10-23 2023-04-11 Janssen Pharmaceutica N.V. Derivados de pirazol como inibidores de nik, seu uso no tratamento ou prevenção de câncer e composição farmacêutica que os compreende
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).
HK1258570A1 (zh) 2015-09-30 2019-11-15 Vertex Pharmaceuticals Inc. 使用dna损伤剂及atr抑制剂的组合治疗癌症的方法
JP2022512706A (ja) 2018-10-16 2022-02-07 エフ．ホフマン－ラ ロシュ アーゲー 眼科におけるＡｋｔ阻害剤の使用
TW202136261A (zh) 2018-10-31 2021-10-01 美商基利科學股份有限公司 經取代之6-氮雜苯并咪唑化合物
TWI721623B (zh) 2018-10-31 2021-03-11 美商基利科學股份有限公司 經取代之6-氮雜苯并咪唑化合物
US11453681B2 (en) 2019-05-23 2022-09-27 Gilead Sciences, Inc. Substituted eneoxindoles and uses thereof
IL315848A (en) 2022-03-31 2024-11-01 Astrazeneca Ab Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors in combination with an AKT inhibitor for cancer treatment
WO2024083716A1 (en) 2022-10-17 2024-04-25 Astrazeneca Ab Combinations of a serd for the treatment of cancer
EP4615431A1 (en) 2022-11-11 2025-09-17 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
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
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

Also Published As

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

Similar Documents

Publication Publication Date Title
JP2009516653A (ja) Ａｋｔ活性の阻害剤
US20080255143A1 (en) Inhibitors of Akt Activity
JP5363997B2 (ja) Ａｋｔ活性の阻害剤
JP2009521504A (ja) Ａｋｔ活性阻害剤
US20110160255A1 (en) Inhibitors of akt activity
US20110129455A1 (en) Inhibitors of akt activity
JP2010522770A (ja) Ａｋｔ活性の阻害物質
US20080318947A1 (en) Inhibitors of Akt Activity
US7625890B2 (en) Substituted imidazo[4,5-c]pyridine compounds as Akt inhibitors
US20110098221A1 (en) INHIBITORS OF Akt ACTIVITY
US20110092423A1 (en) INHIBITORS OF Akt ACTIVITY
US20090227616A1 (en) Inhibitors of akt activity
JP2009521490A (ja) 化合物
JP2009515884A (ja) Ａｋｔ活性の阻害剤
WO2008121685A1 (en) Methods of use for inhibitors of akt activity
JP2011525932A (ja) Ａｋｔ活性の阻害剤
CN101506206A (zh) Akt活性抑制剂

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20091022

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20091022

RD04 Notification of resignation of power of attorney

Free format text: JAPANESE INTERMEDIATE CODE: A7424

Effective date: 20120309

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20120710

A02 Decision of refusal

Free format text: JAPANESE INTERMEDIATE CODE: A02

Effective date: 20130423