[go: up one dir, main page]

CO6190528A2 - Inhibidores de la actividad de la akt - Google Patents

Inhibidores de la actividad de la akt

Info

Publication number
CO6190528A2
CO6190528A2 CO09054952A CO09054952A CO6190528A2 CO 6190528 A2 CO6190528 A2 CO 6190528A2 CO 09054952 A CO09054952 A CO 09054952A CO 09054952 A CO09054952 A CO 09054952A CO 6190528 A2 CO6190528 A2 CO 6190528A2
Authority
CO
Colombia
Prior art keywords
aob
alkyl
cycloalkyl
heterocyclyl
alkynyl
Prior art date
Application number
CO09054952A
Other languages
English (en)
Inventor
Michael Kelly Iii
Mark E Layton
Philip E Sanderson
Original Assignee
Merck & Co Inc
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 Merck & Co Inc filed Critical Merck & Co Inc
Publication of CO6190528A2 publication Critical patent/CO6190528A2/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/06Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/06Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D407/00Heterocyclic 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
    • C07D407/02Heterocyclic 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
    • C07D407/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/12Heterocyclic 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
    • C07D471/14Ortho-condensed systems

Landscapes

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

Abstract

1.- Un compuesto de acuerdo con la Fórmula C:en la que: a es 0 ó1; b es 0 ó 1; m es 0, 1 ó 2; p es 0, 1 ó 2; R2 se selecciona independientemente entre: alquilo (C1-C6), alcoxi (C1-C6); CO2H, halo, OH y NH2; El anillo Y es cicloalquilo (C4-C7); R1 se selecciona entre: H, oxo, (C=O)aObalquilo (C1-C10), (C=O)aOb-arilo, (C=O)aObalquenilo (C2-C10), (C=O)aOb alquinilo (C2-C10), CO2H, halo, OH, Obperfluoroalquilo (C1-C6), (C=O)aNR7R8, CN, (C=O)aOb cicloalquilo (C3-C8), S(O)mNR7R8, SH, S(O)m-alquilo (C1-C10) y (C=O)aOb-heterociclilo, dicho alquilo, arilo, alquenilo, alquinilo, cicloalquilo, y heterociclilo está opcionalmente sustituido con uno o más sustituyentes seleccionados entre R6; R6 es: (C=O)aOb alquilo C1-C10, (C=O)aObarilo, alquenilo C2-C10, alquinilo C2-C10, (C=O)aOb heterociclilo, CO2H, halo, CN, OH, Ob perfluoroalquilo C1-C6, Oa(C=O)bNR7R8, oxo, CHO, (N=O)R7R8, S(O)mNR7R8, SH, S(O)m-alquilo (C1-C10) o (C=O)aOb cicloalquilo C3-C8, dicho alquilo, arilo, alquenilo, alquinilo, heterociclilo, y cicloalquilo opcionalmente sustituido con uno o más sustituyentes seleccionados entre R6a; R6a se selecciona entre: (C=O)aOb alquilo (C1-C10), Oa perfluoroalquilo (C1-C3), alquileno (C0-C6) -S(O)mRa, SH, oxo, OH, halo, CN, alquenilo (C2-C10), alquinilo (C2-C10), cicloalquilo (C3-C6), alquileno (C0-C6)-arilo, alquileno (C0-C6)-heterociclilo, alquilen (C0-C6)-N(Rb)2, C(O)Ra, alquilen (C0-C6) -CO2Ra, C(O)H, y alquilen (C0-C6) -CO2H, dicho alquilo, alquenilo, alquinilo, cicloalquilo, arilo, y heterociclilo está opcionalmente sustituido con hasta tres sustituyentes seleccionados entre Rb, OH, alcoxi (C1-C6), halógeno, CO2H, CN, Oa(C=O)b alquilo (C1-C6), oxo, y N(Rb)2; R7 y R8 se seleccionan independientemente entre: H, (C=O)aOb alquilo (C1-C10), (C=O)aOb cicloalquilo (C3-C8), (C=O)aOb-arilo, (CO)aOb-heterociclilo, alquenilo (C2-C10), alquinilo (C2-C10), SH, SO2Ra, y (C=O)aNRb2, dicho alquilo, cicloalquilo, arilo, heterociclilo, alquenilo, y alquinilo está opcionalmente sustituido con uno o más sustituyentes seleccionados entre R6a, o R7 y R8 se pueden tomar juntos con el nitrógeno al que están unidos para formar a heterociclo monocíclico o bicíclico con 3 - 7 miembros en cada anillo conteniendo opcionalmente, además del nitrógeno, uno o dos heteroátomos adicionales seleccionados entre N, O y S, ...
CO09054952A 2006-12-06 2009-05-28 Inhibidores de la actividad de la akt CO6190528A2 (es)

Applications Claiming Priority (3)

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

Publications (1)

Publication Number Publication Date
CO6190528A2 true CO6190528A2 (es) 2010-08-19

Family

ID=39492823

Family Applications (1)

Application Number Title Priority Date Filing Date
CO09054952A CO6190528A2 (es) 2006-12-06 2009-05-28 Inhibidores de la actividad de la akt

Country Status (29)

Country Link
US (3) US7576209B2 (es)
EP (1) EP2104669B1 (es)
JP (2) JP4431636B1 (es)
KR (1) KR101110598B1 (es)
CN (1) CN101600706B (es)
AR (1) AR064010A1 (es)
AU (1) AU2007328286B2 (es)
BR (1) BRPI0719580A2 (es)
CA (1) CA2670760C (es)
CL (1) CL2007003495A1 (es)
CO (1) CO6190528A2 (es)
CR (1) CR10851A (es)
EA (1) EA016195B1 (es)
EC (1) ECSP099376A (es)
ES (1) ES2527567T3 (es)
GE (1) GEP20125469B (es)
GT (1) GT200900146A (es)
HN (1) HN2009001112A (es)
IL (2) IL198826A (es)
MA (1) MA31027B1 (es)
MX (1) MX2009006052A (es)
NI (1) NI200900106A (es)
NO (1) NO20092569L (es)
NZ (2) NZ595829A (es)
PE (1) PE20081341A1 (es)
SV (1) SV2009003283A (es)
TN (1) TN2009000224A1 (es)
TW (1) TWI386410B (es)
WO (2) WO2008070016A2 (es)

Families Citing this family (56)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HRP20130429T1 (en) * 2005-06-10 2013-06-30 Merck Sharp & Dohme Corp. Inhibitors of akt activity
AR064010A1 (es) * 2006-12-06 2009-03-04 Merck & Co Inc Inhibidores de la actividad de la akt
US20100022573A1 (en) * 2006-12-06 2010-01-28 Layton Mark E Inhibitors of akt activity
US20100048524A1 (en) 2008-03-14 2010-02-25 Angela Brodie Novel C-17-Heteroaryl Steroidal CYP17 Inhibitors/Antiandrogens;Synthesis In Vitro Biological Activities, Pharmacokinetics and Antitumor Activity
US8536193B2 (en) * 2008-06-03 2013-09-17 Merck Sharp & Dohme Corp. Inhibitors of AKT 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
CA2729412A1 (en) 2008-07-04 2010-01-07 Banyu Pharmaceutical Co., Ltd. Novel spirochromanone carboxylic acids
JP5555236B2 (ja) * 2008-08-25 2014-07-23 アイアールエム・リミテッド・ライアビリティ・カンパニー ヘッジホッグ経路モジュレーター
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
CA2750051A1 (en) * 2009-02-02 2010-08-05 Merck Sharp & Dohme Corp. Inhibitors of akt activity
CN102686600A (zh) 2009-02-05 2012-09-19 托凯药业股份有限公司 甾体cyp17抑制剂/抗雄激素物质的新型药物前体
WO2010101734A1 (en) 2009-03-06 2010-09-10 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
EP2413932A4 (en) * 2009-04-01 2012-09-19 Merck Sharp & Dohme HAMMER OF ACT ACTIVITY
SG10201405568UA (en) 2009-09-08 2014-11-27 Hoffmann La Roche 4-substituted pyridin-3-yl-carboxamide compounds and methods of use
WO2011033265A1 (en) 2009-09-18 2011-03-24 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
WO2011146710A1 (en) 2010-05-21 2011-11-24 Glaxosmithkline Llc Combination
JP5830094B2 (ja) * 2010-07-12 2015-12-09 バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングBayer Intellectual Property GmbH 置換イミダゾ[1,2−a]ピリミジンおよび−ピリジン
CA2805015A1 (en) 2010-07-13 2012-01-19 Stuart Ince Bicyclic pyrimidines
CA2806655A1 (en) 2010-07-28 2012-02-02 Bayer Intellectual Property Gmbh Substituted imidazo[1,2-b]pyridazines
CA2821777A1 (en) * 2010-12-16 2012-06-21 Bayer Intellectual Property Gmbh Substituted pyrimido[1,2-b]indazoles and their use as modulators of the pi3k/akt pathway
SG191724A1 (en) 2011-01-11 2013-08-30 Glaxosmithkline Llc Combination
CA2830367C (en) 2011-04-06 2016-08-30 Taiho Pharmaceutical Co., Ltd. Novel imidazo-oxazine compound or salt thereof
SI2694510T1 (sl) 2011-04-07 2016-02-29 Bayer Intellectual Property Gmbh Imidazopiridazini kot inhibitorji AKT kinaze
WO2012177852A1 (en) * 2011-06-24 2012-12-27 Arqule, Inc Substituted imidazopyridinyl compounds
KR20190015600A (ko) * 2011-06-24 2019-02-13 아르퀼 인코포레이티드 치환된 이미다조피리디닐-아미노피리딘 화합물
US9408885B2 (en) 2011-12-01 2016-08-09 Vib Vzw Combinations of therapeutic agents for treating melanoma
EP2802586B1 (en) 2012-01-10 2016-05-25 Bayer Intellectual Property GmbH Substituted imidazopyrazines as akt kinase inhibitors
JP6106694B2 (ja) 2012-01-10 2017-04-05 バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングBayer Intellectual Property GmbH Aktキナーゼ阻害剤としての置換ピラゾロピリミジン類
BR112014017683A2 (pt) 2012-01-20 2017-06-27 Univ Louisiana State controle glicêmico intensificado usando ad36e4orf1 e inibidor de akt1
GB201205164D0 (en) 2012-03-23 2012-05-09 Almac Discovery Ltd Pharmaceutical compounds
KR20160128456A (ko) 2012-07-02 2016-11-07 다이호야쿠힌고교 가부시키가이샤 이미다조옥사진 화합물에 의한 항종양 효과 증강제
CA2904170A1 (en) 2013-03-14 2014-09-25 University Of Maryland, Baltimore Androgen receptor down-regulating agents and uses thereof
KR20160099081A (ko) 2013-07-26 2016-08-19 업데이트 파마 인코포레이트 비산트렌의 치료 효과 개선용 조합 방법
JP2016528252A (ja) 2013-08-12 2016-09-15 トーカイ ファーマシューティカルズ, インコーポレイテッド アンドロゲン標的治療を使用する新生物障害の処置のためのバイオマーカー
JP6355724B2 (ja) 2013-10-01 2018-07-11 ノバルティス アーゲー がんを治療するためのアフレセルチブと組み合わせたエンザルタミド
CN105792825A (zh) 2013-10-01 2016-07-20 诺华股份有限公司 组合
WO2015094928A1 (en) * 2013-12-17 2015-06-25 Merck Sharp & Dohme Corp. Liposomal compositions for allosteric akt inhibitors
CA2939121C (en) 2014-01-28 2020-11-24 Mayo Foundation For Medical Education And Research Effective treatment of osteoarthritis, pulmonary disease, ophthalmic disease, and atherosclerosis by removing senescent cells at the site of the disease
WO2015136398A1 (en) 2014-03-12 2015-09-17 Novartis Ag Combination comprising a btk inhibitor and an akt inhibitor
US10022360B2 (en) * 2014-03-17 2018-07-17 Merck Sharp & Dohme Corp. Polymeric nanoparticles and methods of making and using same
ES2772682T3 (es) 2015-02-27 2020-07-08 Taiho Pharmaceutical Co Ltd Cristal de imidazooxazina, composición farmacéutica que contiene dicho cristal, y método de producción de dicho cristal
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
CN118767143A (zh) 2019-12-12 2024-10-15 听治疗有限责任公司 用于预防和治疗听力损失的组合物和方法
KR20230019109A (ko) * 2020-05-08 2023-02-07 조지아뮨 엘엘씨 Akt3 조절제 및 이의 사용 방법
GB2600384A (en) 2020-09-30 2022-05-04 Vaderis Therapeutics Ag Allosteric AKT inhibitors for use in the treatment of hereditary hemorrhagic telangiectasia
US12404348B2 (en) 2021-11-19 2025-09-02 The Brigham And Women's Hospital, Inc. Bifunctional chimeric molecules for labeling of kinases with target binding moieties and methods of use thereof
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

Family Cites Families (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE60227492D1 (de) * 2001-04-10 2008-08-21 Merck & Co Inc Hemmstoffe der akt aktivität
EP1379250A2 (en) * 2001-04-10 2004-01-14 Merck & Co., Inc. A method of treating cancer
US20030187026A1 (en) * 2001-12-13 2003-10-02 Qun Li Kinase inhibitors
CA2481241C (en) * 2002-04-08 2010-07-27 Merck & Co., Inc. Fused quinoxaline derivatives as inhibitors of akt activity
JP4394959B2 (ja) * 2002-04-08 2010-01-06 メルク エンド カムパニー インコーポレーテッド Akt活性の阻害剤
CA2480880C (en) * 2002-04-08 2011-03-22 Merck & Co., Inc. Inhibitors of akt activity
WO2003086394A1 (en) * 2002-04-08 2003-10-23 Merck & Co., Inc. Inhibitors of akt activity
AU2003284981B2 (en) * 2002-10-30 2009-05-28 Merck Sharp & Dohme Corp. Inhibitors of Akt activity
ATE446752T1 (de) * 2003-04-24 2009-11-15 Merck & Co Inc Hemmer der akt aktivität
CN1809354A (zh) * 2003-04-24 2006-07-26 麦克公司 Akt活性抑制剂
JP4673300B2 (ja) * 2003-04-24 2011-04-20 メルク・シャープ・エンド・ドーム・コーポレイション Akt活性の阻害剤
CN1809351A (zh) * 2003-04-24 2006-07-26 麦克公司 Akt活性抑制剂
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
EP2468729B1 (en) * 2003-10-15 2013-12-25 Ube Industries, Ltd. Novel indazole derivative
US7655649B2 (en) * 2004-04-09 2010-02-02 Merck Sharp & Dohme Corp. Inhibitors of Akt activity
CA2561315A1 (en) 2004-04-09 2005-10-27 Merck & Co., Inc. Inhibitors of akt activity
AU2005290081B2 (en) * 2004-08-23 2010-12-02 Merck Sharp & Dohme Corp. Inhibitors of Akt activity
CA2588474A1 (en) * 2004-12-02 2006-06-29 Merck & Co., Inc. Inhibitors of akt activity
WO2006065601A2 (en) 2004-12-15 2006-06-22 Merck & Co., Inc. Inhibitors of akt activity
CA2597456A1 (en) * 2005-02-14 2006-08-31 Merck & Co., Inc. Inhibitors of akt activity
CN101155588A (zh) * 2005-04-12 2008-04-02 默克公司 Akt活性的抑制剂
HRP20130429T1 (en) 2005-06-10 2013-06-30 Merck Sharp & Dohme Corp. Inhibitors of akt activity
JP2009523820A (ja) * 2006-01-23 2009-06-25 アミラ ファーマシューティカルス,インコーポレーテッド 5−リポキシゲナーゼの三環系抑制剤
AR064010A1 (es) * 2006-12-06 2009-03-04 Merck & Co Inc Inhibidores de la actividad de la akt
EP2137177B1 (en) * 2007-04-05 2014-05-07 Amgen, Inc Aurora kinase modulators and method of use

Also Published As

Publication number Publication date
JP2010511703A (ja) 2010-04-15
WO2008070016A2 (en) 2008-06-12
GEP20125469B (en) 2012-04-10
CR10851A (es) 2009-06-25
TN2009000224A1 (en) 2010-10-18
ES2527567T3 (es) 2015-01-26
US7576209B2 (en) 2009-08-18
US20080161317A1 (en) 2008-07-03
IL205220A0 (en) 2011-07-31
IL198826A (en) 2010-11-30
AU2007328286A2 (en) 2009-08-06
HK1137758A1 (en) 2010-08-06
US20110160183A1 (en) 2011-06-30
GT200900146A (es) 2010-04-13
NZ595829A (en) 2013-04-26
CA2670760A1 (en) 2008-06-12
MX2009006052A (es) 2009-06-17
PE20081341A1 (es) 2008-10-19
AU2007328286B2 (en) 2011-01-20
EA200970542A1 (ru) 2009-12-30
TWI386410B (zh) 2013-02-21
NZ577470A (en) 2011-11-25
AR064010A1 (es) 2009-03-04
HN2009001112A (es) 2011-07-22
WO2008070016A3 (en) 2008-09-12
US20090253734A1 (en) 2009-10-08
NI200900106A (es) 2010-01-20
AU2007328286A1 (en) 2008-06-12
CL2007003495A1 (es) 2008-05-30
CN101600706A (zh) 2009-12-09
KR101110598B1 (ko) 2012-03-08
ECSP099376A (es) 2009-07-31
TW200831509A (en) 2008-08-01
WO2008070041A3 (en) 2008-08-28
WO2008070041A2 (en) 2008-06-12
BRPI0719580A2 (pt) 2013-12-17
SV2009003283A (es) 2009-11-09
CA2670760C (en) 2012-01-24
JP4431636B1 (ja) 2010-03-17
EP2104669A2 (en) 2009-09-30
EP2104669B1 (en) 2014-10-15
CN101600706B (zh) 2013-10-16
EA016195B1 (ru) 2012-03-30
KR20090086095A (ko) 2009-08-10
MA31027B1 (fr) 2009-12-01
JP2009298786A (ja) 2009-12-24
US8288407B2 (en) 2012-10-16
JP5364454B2 (ja) 2013-12-11
NO20092569L (no) 2009-07-06

Similar Documents

Publication Publication Date Title
CO6190528A2 (es) Inhibidores de la actividad de la akt
CO5261601A1 (es) Indolilquinolinonas utiles como inhibidores de la tirosinoquinasa
CO6190518A2 (es) Inhibidores de tirosina quinasa
CR11738A (es) Compuestos de pirimidinona pirrolo 3-metil-2-imino fenil sustituidos como inhibidores bace-1, composiciones y su uso
CR20110001A (es) Compuesto heterocíclico y uso del mismo
PE20070189A1 (es) COMPUESTO DE AMINO-5-HETEROARILO (5 MIEMBROS) IMIDAZOLONA Y SU USO PARA MODULACION DE LA ß-SECRETASA
AR078278A1 (es) Antagonistas de la tiazol y oxazol hepcidina, composiciones farmaceuticas que los contienen y uso de los mismos para el tratamiento de anemias y enfermedades asociadas a deficiencias de hierro.
AR072657A1 (es) Compuestos inhibidores de raf y metodos para su uso
PE20091158A1 (es) 5-anilinoimidazopiridinas y metodos de uso
PE20090773A1 (es) Derivados de morfolina pirimidina
AR053120A1 (es) Aminopiridinas como inhibidores de beta secretasa
CO6541645A2 (es) Compuestos de indol y su uso farmaceutico
CR20120053A (es) Compuestos y metodos inhibidores de jak de pirazolopirimidina
ECSP099335A (es) Compuestos heterocíclicos que contienen nitrógeno y métodos de uso de los mismos
NO20081797L (no) Nye solfonylpyrroler som inhibitorer av HDAC
AR084011A1 (es) Compuestos nitrogenados heterociclicos utiles para el tratamiento de infecciones por el virus sincitial respiratorio (rsv), proceso para prepararlos y composiciones farmaceuticas que los contienen
SV2009002865A (es) Uso de oxazolidinonas para el tratamiento y profilaxis de microangiopatias
CL2010001415A1 (es) Compuestos derivados de diazacarbazol, con actividad inhibidora de quinasa; composición farmacéutica que comprende a uno de los compuestos; y uso de la composición farmacéutica en la preparación de medicamentos para la inhibición del crecimiento celular o el tratamiento de un trastorno hiperproliferativo
MX389265B (es) Aminopirimidinas como inhibidores de alk.
AR077080A1 (es) Compuestos de 2,3-dihidro-1h-indeno
EA200971101A1 (ru) Соединения на основе лантибиотиков, обладающие противомикробной активностью
AR066421A1 (es) Compuestos derivados de piridona
PE20110196A1 (es) 5-alquinil-pirimidinas
ECSP109958A (es) Derivados de pirimidina 934
AR052568A1 (es) Derivados de pirazolo -pirimidina como antagonstas de mglur2

Legal Events

Date Code Title Description
FG Application granted