EA200970542A1 - ИНГИБИТОРЫ ДЕЙСТВИЯ Akt - Google Patents

ИНГИБИТОРЫ ДЕЙСТВИЯ Akt

Info

Publication number
EA200970542A1
EA200970542A1 EA200970542A EA200970542A EA200970542A1 EA 200970542 A1 EA200970542 A1 EA 200970542A1 EA 200970542 A EA200970542 A EA 200970542A EA 200970542 A EA200970542 A EA 200970542A EA 200970542 A1 EA200970542 A1 EA 200970542A1
Authority
EA
Eurasian Patent Office
Prior art keywords
akt
action
compounds
action inhibitors
relates
Prior art date
Application number
EA200970542A
Other languages
English (en)
Other versions
EA016195B1 (ru
Inventor
Майкл Дж. Келли III
Марк Э. Лейтон
Филип Е. Сандерсон
Original Assignee
Мерк Энд Ко., Инк.
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 Мерк Энд Ко., Инк. filed Critical Мерк Энд Ко., Инк.
Publication of EA200970542A1 publication Critical patent/EA200970542A1/ru
Publication of EA016195B1 publication Critical patent/EA016195B1/ru

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
    • C07D407/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D471/12—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 three hetero rings
    • C07D471/14—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Oncology (AREA)
  • Biomedical Technology (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Vascular Medicine (AREA)
  • Emergency Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Transplantation (AREA)
  • Hospice & Palliative Care (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Psychiatry (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)

Abstract

Рассматриваемое изобретение относится к замещенным соединениям нафтиридина, которые ингибируют действие Akt. В частности, раскрыты соединения, селективно ингибирующие одну или две изоформы Akt. Настоящее изобретение также относится к композициям, содержащим указанные ингибирующие соединения, и к способам ингибирования действия Akt путем введения соединения больному, нуждающемуся в лечении рака.
EA200970542A 2006-12-06 2007-12-03 ИНГИБИТОРЫ ДЕЙСТВИЯ Akt EA016195B1 (ru)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US87319806P 2006-12-06 2006-12-06
US88066107P 2007-01-16 2007-01-16
US96787207P 2007-09-06 2007-09-06
PCT/US2007/024772 WO2008070041A2 (en) 2006-12-06 2007-12-03 Inhibitors of akt activity

Publications (2)

Publication Number Publication Date
EA200970542A1 true EA200970542A1 (ru) 2009-12-30
EA016195B1 EA016195B1 (ru) 2012-03-30

Family

ID=39492823

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200970542A EA016195B1 (ru) 2006-12-06 2007-12-03 ИНГИБИТОРЫ ДЕЙСТВИЯ Akt

Country Status (30)

Country Link
US (3) US7576209B2 (ru)
EP (1) EP2104669B1 (ru)
JP (2) JP4431636B1 (ru)
KR (1) KR101110598B1 (ru)
CN (1) CN101600706B (ru)
AR (1) AR064010A1 (ru)
AU (1) AU2007328286B2 (ru)
BR (1) BRPI0719580A2 (ru)
CA (1) CA2670760C (ru)
CL (1) CL2007003495A1 (ru)
CO (1) CO6190528A2 (ru)
CR (1) CR10851A (ru)
EA (1) EA016195B1 (ru)
EC (1) ECSP099376A (ru)
ES (1) ES2527567T3 (ru)
GE (1) GEP20125469B (ru)
GT (1) GT200900146A (ru)
HK (1) HK1137758A1 (ru)
HN (1) HN2009001112A (ru)
IL (2) IL198826A (ru)
MA (1) MA31027B1 (ru)
MX (1) MX2009006052A (ru)
NI (1) NI200900106A (ru)
NO (1) NO20092569L (ru)
NZ (2) NZ577470A (ru)
PE (1) PE20081341A1 (ru)
SV (1) SV2009003283A (ru)
TN (1) TN2009000224A1 (ru)
TW (1) TWI386410B (ru)
WO (2) WO2008070016A2 (ru)

Families Citing this family (54)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX2007015578A (es) * 2005-06-10 2008-03-06 Merck & Co Inc Inhibidores de la actividad akt.
AR064010A1 (es) * 2006-12-06 2009-03-04 Merck & Co Inc Inhibidores de la actividad de la akt
EP2120951A4 (en) * 2006-12-06 2012-02-15 Merck Sharp & Dohme INHIBITORS OF AKT ACTIVITY
US20100048914A1 (en) 2008-03-14 2010-02-25 Angela Brodie Novel C-17-Heteroaryl Steroidal Cyp17 Inhibitors/Antiandrogens, In Vitro Biological Activities, Pharmacokinetics and Antitumor Activity
US8207169B2 (en) * 2008-06-03 2012-06-26 Msd K.K. Substituted [1,2,4]triazolo[4′,3′:1,6]pyrido[2,3-b]pyrazines of the formula D
EP2299825B1 (en) * 2008-06-03 2013-07-31 Merck Sharp & Dohme Corp. Inhibitors of akt activity
CA2729412A1 (en) 2008-07-04 2010-01-07 Banyu Pharmaceutical Co., Ltd. Novel spirochromanone carboxylic acids
BRPI0917936A2 (pt) * 2008-08-25 2017-07-11 Irm Llc Moduladores de via hedgehog
DE102008043724A1 (de) * 2008-11-13 2010-05-20 Biotronik Vi Patent Ag Erhöhung der Effizienz pharmazeutische Wirkstoffe-freisetzender Medizinprodukte durch Kombination mit einem Inhibitor des Transportproteins P-Glycoprotein
WO2010088177A1 (en) * 2009-02-02 2010-08-05 Merck Sharp & Dohme Corp. Inhibitors of akt activity
EP3023433A1 (en) 2009-02-05 2016-05-25 Tokai Pharmaceuticals, Inc. Novel prodrugs of steroidal cyp17 inhibitors/antiandrogens
EP2403339B1 (en) * 2009-03-06 2017-01-18 Merck Sharp & Dohme Corp. Combination cancer therapy with an akt inhibitor and other anticancer agents
WO2010104705A1 (en) 2009-03-12 2010-09-16 Merck Sharp & Dohme Corp. Inhibitors of akt activity
WO2010114780A1 (en) 2009-04-01 2010-10-07 Merck Sharp & Dohme Corp. Inhibitors of akt activity
CN102625807B (zh) 2009-09-08 2016-03-09 霍夫曼-拉罗奇有限公司 4-取代的吡啶-3-基-甲酰胺化合物和使用方法
EP2473495A1 (en) 2009-09-18 2012-07-11 Almac Discovery Limited Pharmaceutical compounds
GB0919380D0 (en) 2009-11-04 2009-12-23 Almac Discovery Ltd Pharmaceutical compouds
GB0922589D0 (en) 2009-12-23 2010-02-10 Almac Discovery Ltd Pharmaceutical compounds
WO2011130921A1 (en) * 2010-04-23 2011-10-27 Merck Sharp & Dohme Corp. Inhibitors of akt activity
JP2013526578A (ja) 2010-05-21 2013-06-24 グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー 組合せ
CA2804845A1 (en) * 2010-07-12 2012-01-19 Stuart Ince Substituted imidazo[1,2-a]pyrimidines and -pyridines
CA2805015A1 (en) 2010-07-13 2012-01-19 Stuart Ince Bicyclic pyrimidines
WO2012013713A2 (en) 2010-07-28 2012-02-02 Bayer Pharma Aktiengesellschaft Substituted imidazo[1,2-b]pyridazines
CN103370321B (zh) * 2010-12-16 2015-07-29 拜耳知识产权有限责任公司 取代的嘧啶并[1,2-b]吲唑及其作为PI3K/AKT途径的调节剂的用途
SG10201600077RA (en) * 2011-01-11 2016-02-26 Glaxosmithkline Llc Combination
MY163187A (en) 2011-04-06 2017-08-15 Taiho Pharmaceutical Co Ltd Novel imidazo-oxazine compound or salt thereof
CN103596957B (zh) 2011-04-07 2016-12-07 拜耳知识产权有限责任公司 作为akt激酶抑制剂的咪唑并哒嗪
CA2837727C (en) * 2011-06-24 2019-12-03 Arqule, Inc. Substituted imidazopyridinyl-aminopyridine compounds
US8815854B2 (en) 2011-06-24 2014-08-26 Arqule, Inc. Substituted imidazopyridinyl compounds
US9408885B2 (en) 2011-12-01 2016-08-09 Vib Vzw Combinations of therapeutic agents for treating melanoma
CN104066735B (zh) 2012-01-10 2016-08-31 拜耳知识产权有限责任公司 作为akt激酶抑制剂的取代的咪唑并吡嗪
US9370517B2 (en) 2012-01-10 2016-06-21 Bayer Intellectual Property Gmbh Substituted pyrazolopyrimidines as Akt kinase inhibitors
EP2804616B1 (en) 2012-01-20 2018-07-18 Board of Supervisors of Louisiana State University and Agricultural and Mechanical College Enhanced glycemic control using ad36e4orf1 and akt1 inhibitor
GB201205164D0 (en) 2012-03-23 2012-05-09 Almac Discovery Ltd Pharmaceutical compounds
HUE036188T2 (hu) 2012-07-02 2018-06-28 Taiho Pharmaceutical Co Ltd Egy imidazooxazin vegyületet tartalmazó tumorellenes hatás potenciátor
EP2968370A4 (en) 2013-03-14 2016-09-21 Univ Maryland AGENT FOR ANDROGEN RECEPTOR DOWNWARD CONTROL AND USES THEREOF
CA2938626A1 (en) 2013-07-26 2015-01-29 John Rothman Compositions to improve the therapeutic benefit of bisantrene
BR112016002970A2 (pt) 2013-08-12 2017-09-12 Tokai Pharmaceuticals Inc biomarcadores para o tratamento de distúrbios neoplásicos que usa terapias direcionadas ao androgênio
RU2016116915A (ru) 2013-10-01 2017-11-13 Новартис Аг Комбинация
CA2923899A1 (en) 2013-10-01 2015-04-09 Novartis Ag Enzalutamide in combination with afuresertib for the treatment of cancer
WO2015094928A1 (en) * 2013-12-17 2015-06-25 Merck Sharp & Dohme Corp. Liposomal compositions for allosteric akt inhibitors
RU2716256C2 (ru) 2014-01-28 2020-03-11 Бак Инститьют Фо Ресеч Он Эйджинг Способы и композиции для уничтожения стареющих клеток и для лечения заболеваний и расстройств, ассоциированных со старением
AU2015228475B9 (en) 2014-03-12 2017-09-21 Novartis Ag Combination comprising a BTK inhibitor and an AKT inhibitor
EP3119395B1 (en) * 2014-03-17 2021-04-28 Merck Sharp & Dohme Corp. Polymeric nanoparticles and methods of making and using same
CN111943962A (zh) 2015-02-27 2020-11-17 大鹏药品工业株式会社 咪唑并噁嗪晶体、含有所述晶体的药物组合物和制备所述晶体的方法
FR3033499A1 (fr) 2015-03-11 2016-09-16 Centre Leon-Berard Composition pour le traitement des tumeurs neuroendocrines pancreatiques
EP3372601B1 (en) 2015-10-22 2022-09-21 Mitsubishi Tanabe Pharma Corporation Novel bicyclic heterocyclic compound
US11883404B2 (en) 2016-03-04 2024-01-30 Taiho Pharmaceuticals Co., Ltd. Preparation and composition for treatment of malignant tumors
WO2017156350A1 (en) 2016-03-09 2017-09-14 K-Gen, Inc. Methods of cancer treatment
CN108426971B (zh) * 2018-03-09 2020-03-20 浙江中一检测研究院股份有限公司 一种快速检测水中微囊藻毒素的方法
WO2019221755A1 (en) 2018-05-18 2019-11-21 Bioventures, Llc Piperlongumine analogues and uses thereof
EP4073102A4 (en) 2019-12-12 2024-05-08 Ting Therapeutics LLC COMPOSITIONS AND METHODS FOR PREVENTION AND TREATMENT OF HEARING LOSS
BR112022022327A2 (pt) * 2020-05-08 2023-01-03 Georgiamune Llc Moduladores de akt3 e métodos de uso dos mesmos
WO2024083716A1 (en) 2022-10-17 2024-04-25 Astrazeneca Ab Combinations of a serd for the treatment of cancer

Family Cites Families (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002083064A2 (en) * 2001-04-10 2002-10-24 Merck & Co., Inc. A method of treating cancer
WO2002083138A1 (en) 2001-04-10 2002-10-24 Merck & Co., Inc. Inhibitors of akt activity
US20030187026A1 (en) 2001-12-13 2003-10-02 Qun Li Kinase inhibitors
CA2480880C (en) 2002-04-08 2011-03-22 Merck & Co., Inc. Inhibitors of akt activity
US20050182256A1 (en) 2002-04-08 2005-08-18 Duggan Mark E. Inhibitors of akt activity
CA2480800C (en) 2002-04-08 2008-09-23 Mark T. Bilodeau Inhibitors of akt activity
AU2003226271B2 (en) 2002-04-08 2007-10-18 Merck Sharp & Dohme Corp. Fused quinoxaline derivatives as inhibitors of Akt activity
EP1558586B1 (en) 2002-10-30 2011-03-30 Merck Sharp & Dohme Corp. Inhibitors of akt activity
WO2004096129A2 (en) 2003-04-24 2004-11-11 Merck & Co., Inc. Inhibitors of akt activity
DE602004023838D1 (de) 2003-04-24 2009-12-10 Merck & Co Inc Hemmer der akt aktivität
US7579355B2 (en) 2003-04-24 2009-08-25 Merck & Co., Inc. Inhibitors of Akt activity
US7638530B2 (en) * 2003-04-24 2009-12-29 Merck & Co., Inc. Inhibitors of Akt activity
WO2005007099A2 (en) 2003-07-10 2005-01-27 Imclone Systems Incorporated Pkb inhibitors as anti-tumor agents
JP2007008816A (ja) * 2003-10-15 2007-01-18 Ube Ind Ltd 新規イソキノリン誘導体
ES2426288T3 (es) * 2003-10-15 2013-10-22 Ube Industries, Ltd. Novedoso derivado de imidazol
CA2561311A1 (en) 2004-04-09 2005-10-27 Merck & Co., Inc. Inhibitors of akt activity
AU2005233569B2 (en) 2004-04-09 2010-08-19 Merck Sharp & Dohme Corp. Inhibitors of Akt activity
US7544677B2 (en) 2004-08-23 2009-06-09 Merck & Co., Inc. Inhibitors of Akt activity
US20080015212A1 (en) 2004-12-02 2008-01-17 Barnett Stanley F Inhibitors Of Akt Activity
CN101242834A (zh) 2004-12-15 2008-08-13 默克公司 Akt活性抑制剂
CN101115479A (zh) 2005-02-14 2008-01-30 默克公司 Akt活性抑制剂
AU2006235314B2 (en) * 2005-04-12 2011-01-20 Merck Sharp & Dohme Corp. Inhibitors of Akt activity
MX2007015578A (es) 2005-06-10 2008-03-06 Merck & Co Inc Inhibidores de la actividad akt.
CA2636043A1 (en) * 2006-01-23 2007-08-02 Amira Pharmaceuticals, Inc. Tricyclic inhibitors of 5-lipoxygenase
AR064010A1 (es) * 2006-12-06 2009-03-04 Merck & Co Inc Inhibidores de la actividad de la akt
US7776857B2 (en) * 2007-04-05 2010-08-17 Amgen Inc. Aurora kinase modulators and method of use

Also Published As

Publication number Publication date
NZ577470A (en) 2011-11-25
IL198826A (en) 2010-11-30
US7576209B2 (en) 2009-08-18
ECSP099376A (es) 2009-07-31
GEP20125469B (en) 2012-04-10
GT200900146A (es) 2010-04-13
JP5364454B2 (ja) 2013-12-11
WO2008070016A2 (en) 2008-06-12
EP2104669A2 (en) 2009-09-30
AU2007328286B2 (en) 2011-01-20
CA2670760C (en) 2012-01-24
SV2009003283A (es) 2009-11-09
WO2008070041A3 (en) 2008-08-28
CN101600706B (zh) 2013-10-16
KR20090086095A (ko) 2009-08-10
AU2007328286A1 (en) 2008-06-12
NO20092569L (no) 2009-07-06
US20080161317A1 (en) 2008-07-03
JP2009298786A (ja) 2009-12-24
TN2009000224A1 (en) 2010-10-18
PE20081341A1 (es) 2008-10-19
EA016195B1 (ru) 2012-03-30
CL2007003495A1 (es) 2008-05-30
TW200831509A (en) 2008-08-01
CN101600706A (zh) 2009-12-09
WO2008070016A3 (en) 2008-09-12
ES2527567T3 (es) 2015-01-26
WO2008070041A2 (en) 2008-06-12
EP2104669B1 (en) 2014-10-15
TWI386410B (zh) 2013-02-21
NI200900106A (es) 2010-01-20
CR10851A (es) 2009-06-25
CO6190528A2 (es) 2010-08-19
IL205220A0 (en) 2011-07-31
HK1137758A1 (en) 2010-08-06
CA2670760A1 (en) 2008-06-12
AR064010A1 (es) 2009-03-04
MA31027B1 (fr) 2009-12-01
HN2009001112A (es) 2011-07-22
KR101110598B1 (ko) 2012-03-08
US20110160183A1 (en) 2011-06-30
MX2009006052A (es) 2009-06-17
JP4431636B1 (ja) 2010-03-17
US8288407B2 (en) 2012-10-16
US20090253734A1 (en) 2009-10-08
AU2007328286A2 (en) 2009-08-06
BRPI0719580A2 (pt) 2013-12-17
JP2010511703A (ja) 2010-04-15
NZ595829A (en) 2013-04-26

Similar Documents

Publication Publication Date Title
EA200970542A1 (ru) ИНГИБИТОРЫ ДЕЙСТВИЯ Akt
WO2006135627A3 (en) Inhibitors of akt activity
WO2006091395A3 (en) Inhibitors of akt activity
WO2006110638A3 (en) Inhibitors of akt activity
UA107783C2 (en) Isoindoline compounds for use in treating cancer
EP4285906A3 (en) Amine-substituted heterocyclic compounds as ehmt2 inhibitors and methods of use thereof
WO2006106326A8 (en) Substituted heterocycles and their use as chk1, pdk1 and pak inhibitors
MA33803B1 (fr) Inhibiteur de bromodomaine de benzodiazépine
EA201170531A1 (ru) Соединения на основе пиридина и пиримидина в качестве ингибиторов сигнального пути wnt для лечения рака
WO2007095124A3 (en) Benzazole derivatives, compositions, and methods of use as aurora kinase inhibitors
PH12013500913A1 (en) Substituted-quinoxaline-type-piperidine compounds and the uses thereof
EA200901032A1 (ru) Соединения и композиции в качестве модуляторов активности gpr119
WO2006135604A3 (en) Inhibitors of checkpoint kinases
MX2012000709A (es) Inhibidores de pirrolopiridina de cinasas.
EA200900571A1 (ru) Композиции chk1 ингибиторов
EA200970486A1 (ru) Соединения для ингибирования митоза
WO2007059154A3 (en) Treatment of cancers with acquired resistance to kit inhibitors
WO2006068796A3 (en) Inhibitors of akt activity
WO2008148074A3 (en) Inhibitors of mtor and methods of treatment using same
TNSN08370A1 (en) Tetrahydropyridothienopyrimidine compounds and methods of use thereof
WO2007008502A3 (en) Inhibitors of checkpoint kinases
WO2007084135A3 (en) Inhibitors of checkpoint kinases
WO2007081572A3 (en) Inhibitors of checkpoint kinases
WO2006074281A3 (en) Inhibitors of checkpoint kinases
EA200901062A1 (ru) Использование ингибиторов растворимой эпоксидгидролазы для предотвращения и лечения метаболического синдрома и соответствующих расстройств

Legal Events

Date Code Title Description
PD4A Registration of transfer of a eurasian patent in accordance with the succession in title
MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ KG MD TJ TM

MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): BY KZ

MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): RU