CA2629429A1 - Inhibitors of akt activity - Google Patents

Inhibitors of akt activity Download PDF

Info

Publication number
CA2629429A1
CA2629429A1 CA002629429A CA2629429A CA2629429A1 CA 2629429 A1 CA2629429 A1 CA 2629429A1 CA 002629429 A CA002629429 A CA 002629429A CA 2629429 A CA2629429 A CA 2629429A CA 2629429 A1 CA2629429 A1 CA 2629429A1
Authority
CA
Canada
Prior art keywords
methyl
compound
pharmaceutically acceptable
ethyl
oxy
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.)
Abandoned
Application number
CA002629429A
Other languages
English (en)
French (fr)
Inventor
Dirk A. Heerding
Tammy J. Clark
Jack Dale Leber
Igor Safonov
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
Individual
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 Individual filed Critical Individual
Publication of CA2629429A1 publication Critical patent/CA2629429A1/en
Abandoned 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)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (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)
  • 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)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CA002629429A 2005-11-10 2006-11-09 Inhibitors of akt activity Abandoned CA2629429A1 (en)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US73595505P 2005-11-10 2005-11-10
US60/735,955 2005-11-10
US77228906P 2006-02-10 2006-02-10
US60/772,289 2006-02-10
US82692806P 2006-09-26 2006-09-26
US60/826,928 2006-09-26
PCT/US2006/043513 WO2007058850A2 (en) 2005-11-10 2006-11-09 Inhibitors of akt activity

Publications (1)

Publication Number Publication Date
CA2629429A1 true CA2629429A1 (en) 2007-05-24

Family

ID=38049129

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002629429A Abandoned CA2629429A1 (en) 2005-11-10 2006-11-09 Inhibitors of akt activity

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)

Families Citing this family (58)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007058852A2 (en) * 2005-11-10 2007-05-24 Smithkline Beecham Corporation Inhibitors of akt activity
SG10201704689XA (en) 2008-01-18 2017-07-28 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
AU2009263037B2 (en) * 2008-06-26 2011-10-06 Amgen Inc. Alkynyl alcohols as kinase inhibitors
KR101712576B1 (ko) 2008-11-10 2017-03-06 버텍스 파마슈티칼스 인코포레이티드 Atr 키나제의 억제제로서 유용한 화합물
PL3354650T3 (pl) 2008-12-19 2022-06-13 Vertex Pharmaceuticals Incorporated Związki przydatne jako inhibitory kinazy atr
JP5836367B2 (ja) 2010-05-12 2015-12-24 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Vertex Pharmaceuticals Incorporated Atrキナーゼ阻害剤として有用な化合物
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
US8962631B2 (en) 2010-05-12 2015-02-24 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
WO2011143423A2 (en) 2010-05-12 2011-11-17 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
US9096584B2 (en) 2010-05-12 2015-08-04 Vertex Pharmaceuticals Incorporated Compounds 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
JP2013529643A (ja) 2010-06-23 2013-07-22 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ロロピラジン誘導体
CA2806304A1 (en) 2010-07-23 2012-01-26 President And Fellows Of Harvard College Methods of detecting prenatal or pregnancy-related diseases or conditions
MX2013000917A (es) * 2010-07-23 2013-07-05 Harvard College Metodos para detectar las enfermedades o condiciones usando celulas fagociticas.
AU2011280997A1 (en) 2010-07-23 2013-02-28 President And Fellows Of Harvard College Methods of detecting autoimmune or immune-related diseases or conditions
AR085908A1 (es) 2011-03-16 2013-11-06 Hoffmann La Roche DERIVADOS DE 3-BUTIN-2-OL Y DE CARBONITRILO CON ACTIVIDAD INHIBIDORA DE LA QUINASA INDUCTORA DE NF-kB (NIK)
CA2832100A1 (en) 2011-04-05 2012-10-11 Vertex Pharmaceuticals Incorporated Aminopyrazine compounds useful as inhibitors of tra kinase
WO2012178123A1 (en) 2011-06-22 2012-12-27 Vertex Pharmaceuticals Incorporated 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
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
AU2012315384B2 (en) 2011-09-30 2017-08-10 Vertex Pharmaceuticals Incorporated Treating pancreatic cancer and non-small cell lung cancer with ATR inhibitors
US8853217B2 (en) 2011-09-30 2014-10-07 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
IN2014KN00943A (enExample) 2011-09-30 2015-08-21 Vertex Pharma
US8765751B2 (en) 2011-09-30 2014-07-01 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
RU2018147217A (ru) 2011-09-30 2019-01-18 Вертекс Фармасьютикалз Инкорпорейтед Способы получения соединений, которые можно использовать в качестве ингибиторов киназы atr
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
WO2013071090A1 (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
EP2776429A1 (en) 2011-11-09 2014-09-17 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
CN104582795B (zh) 2012-04-05 2018-04-20 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
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
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
EP4001275B1 (en) * 2013-06-26 2024-11-27 Helmholtz Zentrum München Deutsches Forschungszentrum für Gesundheit und Umwelt GmbH (s)-enantiomer of mepazine as paracaspase (malt1) inhibitor for the treatment of cancer
AU2014293013A1 (en) 2013-07-26 2016-03-17 Race Oncology Ltd. Combinatorial methods to improve the therapeutic benefit of bisantrene
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
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
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
ES2777608T3 (es) 2014-06-05 2020-08-05 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 útiles como inhibidores de ATR cinasa, la preparación de dicho compuesto y diferentes formas sólidas del mismo
US11179394B2 (en) 2014-06-17 2021-11-23 Vertex Pharmaceuticals Incorporated Method for treating cancer using a combination of Chk1 and ATR inhibitors
WO2016062792A1 (en) 2014-10-23 2016-04-28 Janssen Pharmaceutica Nv New compounds as nik inhibitors
EA033237B1 (ru) 2014-10-23 2019-09-30 Янссен Фармацевтика Нв Новые производные пиразолопиримидина в качестве ингибиторов nik, фармацевтическая композиция и лекарственное средство, содержащее ее
JP6616411B2 (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. 新規な、nik阻害剤としてのピラゾール誘導体
AU2015334914B2 (en) 2014-10-23 2019-09-19 Janssen Pharmaceutica Nv New thienopyrimidine derivatives as NIK inhibitors
US11464774B2 (en) 2015-09-30 2022-10-11 Vertex Pharmaceuticals Incorporated Method for treating cancer using a combination of DNA damaging agents and ATR inhibitors
WO2020078865A1 (en) 2018-10-16 2020-04-23 F. Hoffmann-La Roche Ag Use of akt inhibitors in ophthalmology
EP3873608A1 (en) 2018-10-31 2021-09-08 Gilead Sciences, Inc. Substituted 6-azabenzimidazole compounds having hpk1 inhibitory activity
EP4371987B9 (en) 2018-10-31 2025-11-26 Gilead Sciences, Inc. Substituted 6-azabenzimidazole compounds as hpk1 inhibitors
US11453681B2 (en) 2019-05-23 2022-09-27 Gilead Sciences, Inc. Substituted eneoxindoles and uses thereof
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
WO2024083716A1 (en) 2022-10-17 2024-04-25 Astrazeneca Ab Combinations of a serd for the treatment of cancer
JP2025539034A (ja) 2022-11-11 2025-12-03 アストラゼネカ・アクチエボラーグ 癌の治療のための併用療法

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW200523262A (en) * 2003-07-29 2005-07-16 Smithkline Beecham Corp Inhibitors of AKT activity

Also Published As

Publication number Publication date
AU2006315805A1 (en) 2007-05-24
US20100056523A1 (en) 2010-03-04
EA200801301A1 (ru) 2009-02-27
KR20080067646A (ko) 2008-07-21
TW200736260A (en) 2007-10-01
JP2009516653A (ja) 2009-04-23
IL190968A0 (en) 2009-02-11
WO2007058850A3 (en) 2009-04-30
AP2008004442A0 (en) 2008-04-30
EP1948188A2 (en) 2008-07-30
MA29935B1 (fr) 2008-11-03
ECSP088425A (es) 2008-06-30
AR056786A1 (es) 2007-10-24
EP1948188A4 (en) 2011-02-16
WO2007058850A2 (en) 2007-05-24
NO20082414L (no) 2008-08-05
BRPI0618309A2 (pt) 2011-08-23

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Legal Events

Date Code Title Description
FZDE Discontinued