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DOP2011000129A - 1h-imidazol-2-il-piperidin-1-il como inhibidores de cinasa akt y p70 s6 - Google Patents

1h-imidazol-2-il-piperidin-1-il como inhibidores de cinasa akt y p70 s6

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Publication number
DOP2011000129A
DOP2011000129A DO2011000129A DO2011000129A DOP2011000129A DO P2011000129 A DOP2011000129 A DO P2011000129A DO 2011000129 A DO2011000129 A DO 2011000129A DO 2011000129 A DO2011000129 A DO 2011000129A DO P2011000129 A DOP2011000129 A DO P2011000129A
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Dominican Republic
Prior art keywords
formula
compounds
cancer
present
kinase inhibitors
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Application number
DO2011000129A
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English (en)
Inventor
Sajan Joseph
Robert Dean Dally
Timothy Alan Shepherd
Original Assignee
Lilly Co Eli
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Publication date
Application filed by Lilly Co Eli filed Critical Lilly Co Eli
Publication of DOP2011000129A publication Critical patent/DOP2011000129A/es

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    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-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
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
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    • C07ORGANIC CHEMISTRY
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
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  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

La presente invención se refiere a inhibidores de cinasa p70 S6 y AKT de la fórmula: Fórmula I caracterizado porque es [5-(4-etil-piperazin-1-ilmetil)-piridin-2-il]-[5-fluoro-4-(7-fluoro-3-isopropil-2-metil-3H-benzoimidazol-5-il)-pirimidin-2-il]-amina. La presente invención también proporciona composiciones farmacéuticas que comprenden compuestos de Fórmula I, usos de compuestos de Fórmula I y métodos para usar compuestos de Fórmula I. Los compuestos de la presente invención son útiles en el tratamiento de cáncer, particularmente cáncer colorectal, cáncer de mama, cáncer de pulmón, especialmente cáncer de pulmón de células no pequeñas (NSCLC), cáncer de próstata, gioblastoma, linfoma de células del manto (MCL), leucemia mieloide crónica (CML) y leucemia mieloide aguda (AML).
DO2011000129A 2008-11-11 2011-05-09 1h-imidazol-2-il-piperidin-1-il como inhibidores de cinasa akt y p70 s6 DOP2011000129A (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US11327308P 2008-11-11 2008-11-11

Publications (1)

Publication Number Publication Date
DOP2011000129A true DOP2011000129A (es) 2016-02-29

Family

ID=41402451

Family Applications (1)

Application Number Title Priority Date Filing Date
DO2011000129A DOP2011000129A (es) 2008-11-11 2011-05-09 1h-imidazol-2-il-piperidin-1-il como inhibidores de cinasa akt y p70 s6

Country Status (36)

Country Link
US (1) US8148387B2 (es)
EP (1) EP2358710B1 (es)
JP (1) JP5432275B2 (es)
KR (1) KR101334460B1 (es)
CN (1) CN102216302B (es)
AR (1) AR074072A1 (es)
AU (1) AU2009314324B2 (es)
BR (1) BRPI0921916A2 (es)
CA (1) CA2743019C (es)
CO (1) CO6382114A2 (es)
CR (1) CR20110240A (es)
CY (1) CY1113409T1 (es)
DK (1) DK2358710T3 (es)
DO (1) DOP2011000129A (es)
EA (1) EA018947B1 (es)
EC (1) ECSP11011048A (es)
ES (1) ES2391704T3 (es)
HN (1) HN2011001247A (es)
HR (1) HRP20120738T1 (es)
IL (1) IL211940A (es)
JO (1) JO2822B1 (es)
MA (1) MA32776B1 (es)
MX (1) MX2011005000A (es)
MY (1) MY161461A (es)
NZ (1) NZ592062A (es)
PA (1) PA8846901A1 (es)
PE (1) PE20110807A1 (es)
PL (1) PL2358710T3 (es)
PT (1) PT2358710E (es)
RS (1) RS52520B (es)
SI (1) SI2358710T1 (es)
TN (1) TN2011000207A1 (es)
TW (1) TWI422587B (es)
UA (1) UA100190C2 (es)
WO (1) WO2010056563A1 (es)
ZA (1) ZA201102549B (es)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ597579A (en) 2009-07-02 2013-06-28 Sanofi Sa Novel (6-oxo-1, 6-dihydro-pyrimidin-2-yl)-amide derivatives, preparation thereof, and pharmaceutical use thereof as akt(pkb) phosphorylation inhibitors
EP2491032B1 (en) * 2009-10-23 2014-04-16 Eli Lilly and Company Akt inhibitors
PH12013502073A1 (en) 2011-04-07 2014-01-13 Bayer Ip Gmbh Imidazopyridazines as akt kinase inhibitors
JP5695800B2 (ja) * 2011-07-09 2015-04-08 山東軒竹医薬科技有限公司 ジペプチジルペプチダーゼ−iv阻害剤の塩の結晶形i、及びその製造方法並びにその応用
SG2014009278A (en) 2011-09-12 2014-07-30 Merck Patent Gmbh Novel imidazole amines as modulators of kinase activity
HUE034979T2 (en) 2011-09-12 2018-05-02 Merck Patent Gmbh Aminopyrimidine derivatives for use as modulators of kinase activity
AU2013344549B2 (en) * 2012-11-16 2018-03-08 Xiaoling Chen Novel imidazol-piperidinyl derivatives as modulators of kinase activity
US9580443B2 (en) 2012-11-16 2017-02-28 Merck Patent Gmbh Heterocyclic derivatives as modulators of kinase activity
WO2014143612A1 (en) * 2013-03-11 2014-09-18 Merck Patent Gmbh 6-[4-(1 h-imidazol-2-yl)piperidin-1 -yl]pyrimidin-4-amine derivatives as modulators of kinase activity
EP3105224A1 (en) * 2014-02-11 2016-12-21 Merck Patent GmbH Pyrimidine imidazole amines as modulators of kinase activity
TW201718574A (zh) 2015-08-12 2017-06-01 美國禮來大藥廠 Cgrp受體拮抗劑
PT3459953T (pt) * 2016-05-20 2021-07-29 Taiho Pharmaceutical Co Ltd Novo derivado de 5h-pirrolo[2,3-d]pirimidin-6(7h)-ona
KR20220154722A (ko) * 2020-03-17 2022-11-22 지앙수 헨그루이 파마슈티컬스 컴퍼니 리미티드 융합된 이환식 유도체, 이의 제조 방법, 및 이의 약학적 용도
CN113444110B (zh) * 2020-03-25 2023-05-12 江苏恒瑞医药股份有限公司 四氢吡咯并吡唑类衍生物、其制备方法及其在医药上的应用
TW202328138A (zh) 2021-09-17 2023-07-16 大陸商江蘇恒瑞醫藥股份有限公司 稠合二環類衍生物的可藥用鹽、晶型及其製備方法
WO2024009977A1 (ja) * 2022-07-05 2024-01-11 大鵬薬品工業株式会社 5H-ピロロ[2,3-d]ピリミジン-6(7H)-オン及びその塩体の結晶

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1750727A2 (en) 2004-04-23 2007-02-14 Exelixis, Inc. Kinase modulators and methods of use
MY179032A (en) 2004-10-25 2020-10-26 Cancer Research Tech Ltd Ortho-condensed pyridine and pyrimidine derivatives (e.g.purines) as protein kinase inhibitors
US7994172B2 (en) 2004-12-28 2011-08-09 Exelixis, Inc. [1H-pyrazolo[3, 4-D]pyrimidin-4-yl]-piperidine or -piperazine compounds as serine-theoronine kinase modulators (P70s6k, Atk1 and Atk2) for the treatment of immunological, inflammatory and proliferative diseases
WO2006091450A1 (en) * 2005-02-18 2006-08-31 Lexicon Genetics Incorporated 4-piperidin-1-yl-7h-pyrrolo[2,3-d]pyrimidine compounds
WO2007003960A1 (en) 2005-06-30 2007-01-11 Prosidion Limited Gpcr agonists
JP5606734B2 (ja) 2006-04-25 2014-10-15 アステックス、セラピューティックス、リミテッド 医薬化合物
JP2009536620A (ja) 2006-04-25 2009-10-15 アステックス、セラピューティックス、リミテッド 医薬組み合わせ物
WO2008012635A2 (en) 2006-07-26 2008-01-31 Pfizer Products Inc. Amine derivatives useful as anticancer agents
AR064416A1 (es) * 2006-12-21 2009-04-01 Cancer Rec Tech Ltd Derivados de purina, piridina y pirimidina condensadas con heterociclos, moduladores de pka y/o pkb, composiciones farmaceuticas que los contienen, y usos para el tratamiento de enfermedades hiperproliferativas.
UA99284C2 (ru) 2007-05-11 2012-08-10 Елі Ліллі Енд Компані ИНГИБИТОРЫ р70 S6-КИНАЗЫ

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CA2743019C (en) 2013-08-13
PL2358710T3 (pl) 2012-12-31
MA32776B1 (fr) 2011-11-01
US20100120801A1 (en) 2010-05-13
BRPI0921916A2 (pt) 2015-12-29
JP2012508274A (ja) 2012-04-05
TN2011000207A1 (en) 2012-12-17
IL211940A0 (en) 2011-06-30
ECSP11011048A (es) 2011-06-30
AU2009314324B2 (en) 2013-06-20
MX2011005000A (es) 2011-05-25
RS52520B (en) 2013-04-30
CY1113409T1 (el) 2016-06-22
PE20110807A1 (es) 2011-10-31
HN2011001247A (es) 2013-05-20
NZ592062A (en) 2013-03-28
CO6382114A2 (es) 2012-02-15
AR074072A1 (es) 2010-12-22
SI2358710T1 (sl) 2012-11-30
TWI422587B (zh) 2014-01-11
EP2358710B1 (en) 2012-08-15
EA201170680A1 (ru) 2011-12-30
CN102216302B (zh) 2013-08-21
AU2009314324A1 (en) 2010-05-20
CA2743019A1 (en) 2010-05-20
IL211940A (en) 2014-01-30
HRP20120738T1 (hr) 2012-10-31
PA8846901A1 (es) 2010-06-28
PT2358710E (pt) 2012-10-01
ES2391704T3 (es) 2012-11-29
ZA201102549B (en) 2012-09-26
JP5432275B2 (ja) 2014-03-05
HK1158203A1 (en) 2012-07-13
CN102216302A (zh) 2011-10-12
EP2358710A1 (en) 2011-08-24
UA100190C2 (en) 2012-11-26
JO2822B1 (en) 2014-09-15
EA018947B1 (ru) 2013-11-29
KR20110074578A (ko) 2011-06-30
KR101334460B1 (ko) 2013-12-02
TW201022268A (en) 2010-06-16
DK2358710T3 (da) 2012-09-03
CR20110240A (es) 2011-06-09
MY161461A (en) 2017-04-14
WO2010056563A1 (en) 2010-05-20
US8148387B2 (en) 2012-04-03

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