TW200736260A - Inhibitors of Akt activity - Google Patents

Inhibitors of Akt activity

Info

Publication number
TW200736260A
TW200736260A TW095141228A TW95141228A TW200736260A TW 200736260 A TW200736260 A TW 200736260A TW 095141228 A TW095141228 A TW 095141228A TW 95141228 A TW95141228 A TW 95141228A TW 200736260 A TW200736260 A TW 200736260A
Authority
TW
Taiwan
Prior art keywords
inhibitors
akt activity
activity
compounds
akt
Prior art date
Application number
TW095141228A
Other languages
English (en)
Inventor
Dirk A Heerding
Tammy J Clark
Jack Dale Leber
Igor Safonov
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 TW200736260A publication Critical patent/TW200736260A/zh

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)
  • 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)
TW095141228A 2005-11-10 2006-11-08 Inhibitors of Akt activity TW200736260A (en)

Applications Claiming Priority (3)

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

Publications (1)

Publication Number Publication Date
TW200736260A true TW200736260A (en) 2007-10-01

Family

ID=38049129

Family Applications (1)

Application Number Title Priority Date Filing Date
TW095141228A TW200736260A (en) 2005-11-10 2006-11-08 Inhibitors of Akt activity

Country Status (16)

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

Families Citing this family (58)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2009517342A (ja) * 2005-11-10 2009-04-30 スミスクライン・ビーチャム・コーポレイション Ａｋｔ活性の阻害剤
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
WO2009138229A1 (en) * 2008-05-16 2009-11-19 Cellzome Ag Methods for the identification of parp interacting molecules and for purification of parp proteins
US20110086834A1 (en) * 2008-06-26 2011-04-14 Amgen Inc. Alkynyl alcohols as kinase inhibitors
EP2370424A1 (en) 2008-11-10 2011-10-05 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
EP4059932A1 (en) 2008-12-19 2022-09-21 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
WO2011143425A2 (en) 2010-05-12 2011-11-17 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
EP2569286B1 (en) 2010-05-12 2014-08-20 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
EP2568984A1 (en) 2010-05-12 2013-03-20 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
WO2011143419A1 (en) 2010-05-12 2011-11-17 Vertex Pharmaceuticals Incorporated Pyrazines useful as inhibitors of atr kinase
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
US8623869B2 (en) 2010-06-23 2014-01-07 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
CA2806304A1 (en) 2010-07-23 2012-01-26 President And Fellows Of Harvard College Methods of detecting prenatal or pregnancy-related diseases or conditions
SG10201505724SA (en) * 2010-07-23 2015-09-29 Harvard College Methods of detecting diseases or conditions using phagocytic cells
EP2596116A4 (en) 2010-07-23 2014-03-19 Harvard College METHODS FOR DETECTION OF AUTOIMMUNE OR IMMUNE-RELATED DISEASES / PATHOLOGIES
JP2014508183A (ja) * 2011-03-16 2014-04-03 エフ．ホフマン−ラ ロシュ アーゲー ６，５−複素環式プロパルギルアルコール化合物及びこれらの使用
CA2832100A1 (en) 2011-04-05 2012-10-11 Vertex Pharmaceuticals Incorporated Aminopyrazine compounds useful as inhibitors of tra 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
US8822469B2 (en) 2011-06-22 2014-09-02 Vertex Pharmaceuticals Incorporated Pyrrolo[2,3-B]pyrazines useful as inhibitors of ATR kinase
US20130089626A1 (en) 2011-09-30 2013-04-11 Vertex Pharmaceuticals Incorporated Treating Cancer with ATR Inhibitors
CA2850564A1 (en) 2011-09-30 2013-04-04 Vertex Pharmaceuticals Incorporated 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
ES2751741T3 (es) 2011-09-30 2020-04-01 Vertex Pharma Procedimiento para fabricar compuestos útiles como inhibidores de la quinasa ATR
US8765751B2 (en) 2011-09-30 2014-07-01 Vertex Pharmaceuticals Incorporated 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
WO2013071093A1 (en) 2011-11-09 2013-05-16 Vertex Pharmaceuticals Incorporated Pyrazine compounds useful as inhibitors of atr kinase
US8846918B2 (en) 2011-11-09 2014-09-30 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
EP2776419B1 (en) 2011-11-09 2016-05-11 Vertex Pharmaceuticals Incorporated Pyrazine compounds useful as inhibitors of atr kinase
WO2013071090A1 (en) 2011-11-09 2013-05-16 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
IN2014KN02410A (zh) 2012-04-05 2015-05-01 Vertex Pharma
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
LT3418281T (lt) 2012-12-07 2021-01-11 Vertex Pharmaceuticals Inc. Pirazolo[1,5-a]pirimidinai, naudotini kaip atr kinazės inhibitoriai, skirti vėžinių ligų gydymui
NZ771629A (en) 2013-03-09 2022-12-23 Harry Stylli Methods of detecting cancer
US9663519B2 (en) 2013-03-15 2017-05-30 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
TWI663166B (zh) 2013-04-24 2019-06-21 健生藥品公司 新化合物
EP3013818B1 (en) 2013-06-26 2021-12-29 Helmholtz Zentrum München - Deutsches Forschungszentrum für Gesundheit und Umwelt (GmbH) (s)-enantiomer of mepazine as paracaspase (malt1) inhibitor for treating cancer
KR20160099081A (ko) 2013-07-26 2016-08-19 업데이트 파마 인코포레이트 비산트렌의 치료 효과 개선용 조합 방법
TWI627173B (zh) * 2013-09-26 2018-06-21 比利時商健生藥品公司 作為ＮＩＫ抑制劑的新穎３－（１Ｈ－吡唑－４－基）－１Ｈ－吡咯并［２，３－ｃ］吡啶衍生物
TWI704146B (zh) * 2013-09-26 2020-09-11 比利時商健生藥品公司 用作ＮＩＫ抑制劑之新的1-(４-嘧啶基)-１Ｈ-吡唑並[３,２-ｃ]吡啶衍生物
KR102153886B1 (ko) 2013-12-06 2020-09-09 버텍스 파마슈티칼스 인코포레이티드 Atr 키나제 억제제로서 유용한 2-아미노-6-플루오로-n-[5-플루오로-피리딘-3-일]피라졸로[1,5-a]피리미딘-3-카복스아미드 화합물, 이의 제조 방법, 이의 상이한 고체형 및 방사성표지된 유도체
PT3152212T (pt) 2014-06-05 2020-03-13 Vertex Pharma Derivados radiomarcados de um composto de 2-amino-6-fluoro-n-[5-fluoro-piridin-3-il]-pirazolo[1,5-a]pirimidin-3-carboxamida útil como inibidor de atr quinase, preparação do dito composto e diferentes formas sólidas do mesmo
RU2736219C2 (ru) 2014-06-17 2020-11-12 Вертекс Фармасьютикалз Инкорпорейтед Способ лечения рака с использованием комбинации ингибиторов снк1 и atr
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
CN107074881B (zh) 2014-10-23 2019-07-30 詹森药业有限公司 作为nik抑制剂的新的噻吩并嘧啶衍生物
WO2016062790A1 (en) 2014-10-23 2016-04-28 Janssen Pharmaceutica Nv New pyrazolopyrimidine derivatives as nik inhibitors
ES2718557T3 (es) 2014-10-23 2019-07-02 Janssen Pharmaceutica Nv Nuevos compuestos como inhibidores de nik
KR20180054657A (ko) 2015-09-30 2018-05-24 버텍스 파마슈티칼스 인코포레이티드 Dna 손상제 및 atr 저해제의 병용물을 사용한 암 치료 방법
WO2020078865A1 (en) 2018-10-16 2020-04-23 F. Hoffmann-La Roche Ag Use of akt inhibitors in ophthalmology
MX2021005047A (es) 2018-10-31 2021-09-08 Gilead Sciences Inc Compuestos de 6-azabenzimidazol sustituidos como inhibidores de hpk1.
CN112969505B (zh) 2018-10-31 2023-11-14 吉利德科学公司 具有hpk1抑制活性的取代的6-氮杂苯并咪唑化合物
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
WO2023187037A1 (en) 2022-03-31 2023-10-05 Astrazeneca Ab Epidermal growth factor receptor (egfr) tyrosine kinase inhibitors in combination with an akt inhibitor for the treatment of cancer
WO2024083716A1 (en) 2022-10-17 2024-04-25 Astrazeneca Ab Combinations of a serd for the treatment of cancer
WO2024100236A1 (en) 2022-11-11 2024-05-16 Astrazeneca Ab Combination therapies for the treatment of cancer

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR045134A1 (es) * 2003-07-29 2005-10-19 Smithkline Beecham Plc Compuesto de 1h - imidazo [4,5-c] piridin-ilo, composicion farmaceutica que lo comprende, proceso para prepararla, su uso para preparar dicha composicion farmaceutica, combinacion farmaceutica, uso de la combinacion farmaceutica para la preparacion de un medicamento, procedimientos para preparar dic

Also Published As

Publication number Publication date
AU2006315805A1 (en) 2007-05-24
JP2009516653A (ja) 2009-04-23
CA2629429A1 (en) 2007-05-24
EP1948188A4 (en) 2011-02-16
AP2008004442A0 (en) 2008-04-30
WO2007058850A3 (en) 2009-04-30
MA29935B1 (fr) 2008-11-03
KR20080067646A (ko) 2008-07-21
NO20082414L (no) 2008-08-05
WO2007058850A2 (en) 2007-05-24
EP1948188A2 (en) 2008-07-30
BRPI0618309A2 (pt) 2011-08-23
AR056786A1 (es) 2007-10-24
IL190968A0 (en) 2009-02-11
US20100056523A1 (en) 2010-03-04
ECSP088425A (es) 2008-06-30
EA200801301A1 (ru) 2009-02-27

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