KR101334460B1 - Ａｋｔ 및 ｐ70 ｓ6 키나제 억제제 - Google Patents

Ａｋｔ 및 ｐ70 ｓ6 키나제 억제제 Download PDF

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Publication number
KR101334460B1
KR101334460B1 KR1020117010569A KR20117010569A KR101334460B1 KR 101334460 B1 KR101334460 B1 KR 101334460B1 KR 1020117010569 A KR1020117010569 A KR 1020117010569A KR 20117010569 A KR20117010569 A KR 20117010569A KR 101334460 B1 KR101334460 B1 KR 101334460B1
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phenyl
imidazol
ethyl
equiv
fluoro
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KR20110074578A (ko
Inventor
로버트 딘 달리
사잔 조세프
티모시 알란 셰퍼드
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일라이 릴리 앤드 캄파니
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—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
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • 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
    • 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
    • A61P3/06—Antihyperlipidemics
    • 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
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • 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
    • C07D401/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/32—Nitrogen atom
    • C07D473/34—Nitrogen atom attached in position 6, e.g. adenine

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Neurology (AREA)
  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Oncology (AREA)
  • Neurosurgery (AREA)
  • Pulmonology (AREA)
  • Reproductive Health (AREA)
  • Emergency Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Biomedical Technology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
KR1020117010569A 2008-11-11 2009-11-03 Ａｋｔ 및 ｐ70 ｓ6 키나제 억제제 Expired - Fee Related KR101334460B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US11327308P 2008-11-11 2008-11-11
US61/113,273 2008-11-11
PCT/US2009/063020 WO2010056563A1 (en) 2008-11-11 2009-11-03 Akt and p70 s6 kinase inhibitors

Publications (2)

Publication Number Publication Date
KR20110074578A KR20110074578A (ko) 2011-06-30
KR101334460B1 true KR101334460B1 (ko) 2013-12-02

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KR1020117010569A Expired - Fee Related KR101334460B1 (ko) 2008-11-11 2009-11-03 Ａｋｔ 및 ｐ70 ｓ6 키나제 억제제

Country Status (36)

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

Families Citing this family (16)

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JP5680638B2 (ja) 2009-07-02 2015-03-04 サノフイ 新規な（６−オキソ−１，６−ジヒドロピリミジン−２−イル）アミド誘導体、この調製およびａｋｔ（ｐｋｂ）リン酸化インヒビターとしてのこの医薬的な使用
KR101398268B1 (ko) * 2009-10-23 2014-05-23 일라이 릴리 앤드 캄파니 Ａｋｔ 억제제
EP2694510B1 (en) 2011-04-07 2015-10-14 Bayer Intellectual Property GmbH Imidazopyridazines as akt kinase inhibitors
ES2547687T3 (es) * 2011-07-09 2015-10-08 Xuanzhu Pharma Co., Ltd. Forma cristalina I de sal de un inhibidor de dipeptidil-peptidasa IV y procedimiento de preparación y uso de la misma
SI2755958T1 (sl) 2011-09-12 2017-12-29 Merck Patent Gmbh Aminopirimidinski derivati za uporabo kot modulatorji kinazne aktivnosti
SG10201606301YA (en) * 2011-09-12 2016-09-29 Merck Patent Gmbh Novel imidazole amines as modulators of kinase activity
US9580443B2 (en) 2012-11-16 2017-02-28 Merck Patent Gmbh Heterocyclic derivatives as modulators of kinase activity
ES2807539T3 (es) * 2012-11-16 2021-02-23 Merck Patent Gmbh Derivados de imidazol-piperidinilo como moduladores de la actividad de quinasa
US9458134B2 (en) * 2013-03-11 2016-10-04 Merck Patent Gmbh Heterocycles as modulators of kinase activity
AU2015217397B2 (en) * 2014-02-11 2019-01-17 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
US10538528B2 (en) * 2016-05-20 2020-01-21 Taiho Pahrmaceutical Co., Ltd. 5H-pyrrolo[2,3-D]pyrimidin-6(7H)-one derivative
JP2023520140A (ja) * 2020-03-17 2023-05-16 江蘇恒瑞医薬股▲ふん▼有限公司 縮合二環系誘導体、その調製方法及びその医薬的応用
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
EP4403550A4 (en) 2021-09-17 2025-01-08 Jiangsu Hengrui Pharmaceuticals Co., Ltd. CONDENSED BICYCLIC DERIVATIVE, PHARMACEUTICALLY ACCEPTABLE SALT, CRYSTALLINE FORM THEREOF AND MANUFACTURING PROCESS THEREOF
TW202421127A (zh) * 2022-07-05 2024-06-01 日商大鵬藥品工業股份有限公司 ５Ｈ－吡咯并〔２，３－ｄ〕嘧啶－６（７Ｈ）－酮及其鹽體之結晶

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WO2008075109A1 (en) 2006-12-21 2008-06-26 Astex Therapeutics Limited Substituted piperidines having protein kinase inhibiting activity

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US8076338B2 (en) 2004-04-23 2011-12-13 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
ATE543821T1 (de) 2004-12-28 2012-02-15 Exelixis Inc Ä1h-pyrazoloä3,4-düpyrimidin-4-ylü-piperidin- oder piperazinverbindungen als serin-threonin- kinasemodulatoren (p70s6k, atk1 und atk2) zur behandlung von immunologischen, entzündlichen und proliferativen erkrankungen
US7423043B2 (en) * 2005-02-18 2008-09-09 Lexicon Pharmaceuticals, Inc. 4-Piperidin-1-yl-7H-pyrrolo[2,3-d]pyrimidine compounds
WO2007003960A1 (en) 2005-06-30 2007-01-11 Prosidion Limited Gpcr agonists
DK3421471T3 (da) 2006-04-25 2021-06-14 Astex Therapeutics Ltd Purin- og deazapurinderivater som farmaceutiske forbindelser
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
UA99284C2 (ru) 2007-05-11 2012-08-10 Елі Ліллі Енд Компані ИНГИБИТОРЫ р70 S6-КИНАЗЫ

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008075109A1 (en) 2006-12-21 2008-06-26 Astex Therapeutics Limited Substituted piperidines having protein kinase inhibiting activity

Also Published As

Publication number Publication date
PL2358710T3 (pl) 2012-12-31
ZA201102549B (en) 2012-09-26
AR074072A1 (es) 2010-12-22
JO2822B1 (en) 2014-09-15
PE20110807A1 (es) 2011-10-31
MX2011005000A (es) 2011-05-25
EP2358710A1 (en) 2011-08-24
DOP2011000129A (es) 2016-02-29
TWI422587B (zh) 2014-01-11
US8148387B2 (en) 2012-04-03
TW201022268A (en) 2010-06-16
CO6382114A2 (es) 2012-02-15
DK2358710T3 (da) 2012-09-03
HRP20120738T1 (hr) 2012-10-31
JP5432275B2 (ja) 2014-03-05
HN2011001247A (es) 2013-05-20
EA201170680A1 (ru) 2011-12-30
BRPI0921916A2 (pt) 2015-12-29
AU2009314324B2 (en) 2013-06-20
IL211940A0 (en) 2011-06-30
PA8846901A1 (es) 2010-06-28
EP2358710B1 (en) 2012-08-15
NZ592062A (en) 2013-03-28
CN102216302A (zh) 2011-10-12
US20100120801A1 (en) 2010-05-13
EA018947B1 (ru) 2013-11-29
JP2012508274A (ja) 2012-04-05
CY1113409T1 (el) 2016-06-22
CN102216302B (zh) 2013-08-21
SI2358710T1 (sl) 2012-11-30
KR20110074578A (ko) 2011-06-30
RS52520B (sr) 2013-04-30
AU2009314324A1 (en) 2010-05-20
CR20110240A (es) 2011-06-09
TN2011000207A1 (en) 2012-12-17
IL211940A (en) 2014-01-30
ECSP11011048A (es) 2011-06-30
CA2743019A1 (en) 2010-05-20
ES2391704T3 (es) 2012-11-29
PT2358710E (pt) 2012-10-01
MY161461A (en) 2017-04-14
MA32776B1 (fr) 2011-11-01
HK1158203A1 (en) 2012-07-13
WO2010056563A1 (en) 2010-05-20
UA100190C2 (en) 2012-11-26
CA2743019C (en) 2013-08-13

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