CA2743019C - Akt and p70 s6 kinase inhibitors - Google Patents

Akt and p70 s6 kinase inhibitors Download PDF

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Publication number
CA2743019C
CA2743019C CA2743019A CA2743019A CA2743019C CA 2743019 C CA2743019 C CA 2743019C CA 2743019 A CA2743019 A CA 2743019A CA 2743019 A CA2743019 A CA 2743019A CA 2743019 C CA2743019 C CA 2743019C
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Canada
Prior art keywords
imidazol
fluoro
ethyl
piperidin
pheny1
Prior art date
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Expired - Fee Related
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CA2743019A
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English (en)
French (fr)
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CA2743019A1 (en
Inventor
Robert Dean Dally
Sajan Joseph
Timothy Alan Shepherd
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Eli Lilly and Co
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Eli Lilly and Co
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Expired - Fee Related legal-status Critical Current
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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

Landscapes

  • 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)
  • Physical Education & Sports Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Reproductive Health (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Neurosurgery (AREA)
  • Child & Adolescent Psychology (AREA)
  • Oncology (AREA)
  • Emergency Medicine (AREA)
  • Pulmonology (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)
CA2743019A 2008-11-11 2009-11-03 Akt and p70 s6 kinase inhibitors Expired - Fee Related CA2743019C (en)

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
CA2743019A1 CA2743019A1 (en) 2010-05-20
CA2743019C true CA2743019C (en) 2013-08-13

Family

ID=41402451

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2743019A Expired - Fee Related CA2743019C (en) 2008-11-11 2009-11-03 Akt and p70 s6 kinase inhibitors

Country Status (36)

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

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
AU2010310786B2 (en) * 2009-10-23 2014-03-27 Eli Lilly And Company AKT inhibitors
EA024890B1 (ru) 2011-04-07 2016-10-31 Байер Интеллектчуал Проперти Гмбх Имидазопиридазины в качестве ингибиторов akt киназы
EP2730575B1 (en) * 2011-07-09 2015-09-16 Xuanzhu Pharma Co., Ltd. Crystal form i of salt of dipeptidyl peptidase-iv inhibitor and preparation method and use thereof
SG2014009260A (en) 2011-09-12 2014-09-26 Merck Patent Gmbh Aminopyrimidine derivatives for use as modulators of kinase activity
SI2755965T1 (sl) 2011-09-12 2017-12-29 Merck Patent Gmbh Novi imidazolni amidi kot modulatorji kinazne aktivnosti
ES2807539T3 (es) * 2012-11-16 2021-02-23 Merck Patent Gmbh Derivados de imidazol-piperidinilo como moduladores de la actividad de quinasa
JP6386467B2 (ja) * 2012-11-16 2018-09-05 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングＭｅｒｃｋ Ｐａｔｅｎｔ Ｇｅｓｅｌｌｓｃｈａｆｔ ｍｉｔ ｂｅｓｃｈｒａｅｎｋｔｅｒ Ｈａｆｔｕｎｇ キナーゼ活性のモジュレーターとしての新規複素環式誘導体
SG11201505999VA (en) * 2013-03-11 2015-08-28 Merck Patent Gmbh 6-[4-(1 h-imidazol-2-yl)piperidin-1 -yl]pyrimidin-4-amine derivatives as modulators of kinase activity
CN105980375A (zh) * 2014-02-11 2016-09-28 默克专利有限公司 用作激酶活性调节剂的嘧啶咪唑胺
TW201718574A (zh) 2015-08-12 2017-06-01 美國禮來大藥廠 Ｃｇｒｐ受體拮抗劑
RU2713181C1 (ru) * 2016-05-20 2020-02-04 Тайхо Фармасьютикал Ко., Лтд. Новое производное 5h-пирроло[2,3-d]пиримидин-6(7h)-она
CN118530260A (zh) 2020-03-17 2024-08-23 江苏恒瑞医药股份有限公司 稠合二环类衍生物、其制备方法及其在医药上的应用
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
CA3231865A1 (en) 2021-09-17 2023-03-23 Tingting SHANG Fused bicyclic derivative, pharmaceutically acceptable salt, crystal form thereof and preparation method therefor
MA71401A (fr) * 2022-07-05 2025-04-30 Taiho Pharmaceutical Co., Ltd. 5h-pyrrolo[2,3-d]pyrimidine-6(7h)-one, et cristaux de sel de celui-ci

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005117909A2 (en) 2004-04-23 2005-12-15 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
US20090082370A1 (en) 2006-04-25 2009-03-26 Neil Thomas Thompson Pharmaceutical Combinations of PK Inhibitors and Other Active Agents
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

Also Published As

Publication number Publication date
JO2822B1 (en) 2014-09-15
CY1113409T1 (el) 2016-06-22
DOP2011000129A (es) 2016-02-29
TWI422587B (zh) 2014-01-11
JP2012508274A (ja) 2012-04-05
CN102216302B (zh) 2013-08-21
CO6382114A2 (es) 2012-02-15
AU2009314324A1 (en) 2010-05-20
JP5432275B2 (ja) 2014-03-05
HRP20120738T1 (hr) 2012-10-31
PE20110807A1 (es) 2011-10-31
CR20110240A (es) 2011-06-09
PT2358710E (pt) 2012-10-01
KR101334460B1 (ko) 2013-12-02
ECSP11011048A (es) 2011-06-30
EP2358710B1 (en) 2012-08-15
TN2011000207A1 (en) 2012-12-17
DK2358710T3 (da) 2012-09-03
AR074072A1 (es) 2010-12-22
MY161461A (en) 2017-04-14
HK1158203A1 (en) 2012-07-13
CA2743019A1 (en) 2010-05-20
ES2391704T3 (es) 2012-11-29
PL2358710T3 (pl) 2012-12-31
US8148387B2 (en) 2012-04-03
IL211940A (en) 2014-01-30
CN102216302A (zh) 2011-10-12
IL211940A0 (en) 2011-06-30
BRPI0921916A2 (pt) 2015-12-29
WO2010056563A1 (en) 2010-05-20
PA8846901A1 (es) 2010-06-28
AU2009314324B2 (en) 2013-06-20
EP2358710A1 (en) 2011-08-24
SI2358710T1 (sl) 2012-11-30
HN2011001247A (es) 2013-05-20
NZ592062A (en) 2013-03-28
EA018947B1 (ru) 2013-11-29
EA201170680A1 (ru) 2011-12-30
RS52520B (sr) 2013-04-30
ZA201102549B (en) 2012-09-26
US20100120801A1 (en) 2010-05-13
TW201022268A (en) 2010-06-16
MX2011005000A (es) 2011-05-25
UA100190C2 (en) 2012-11-26
KR20110074578A (ko) 2011-06-30
MA32776B1 (fr) 2011-11-01

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