HRP20120738T1 - Inhibitori kinaza akt i p70 s6 - Google Patents

Inhibitori kinaza akt i p70 s6 Download PDF

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Publication number
HRP20120738T1
HRP20120738T1 HRP20120738AT HRP20120738T HRP20120738T1 HR P20120738 T1 HRP20120738 T1 HR P20120738T1 HR P20120738A T HRP20120738A T HR P20120738AT HR P20120738 T HRP20120738 T HR P20120738T HR P20120738 T1 HRP20120738 T1 HR P20120738T1
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Croatia
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pharmaceutically acceptable
acceptable salt
compound according
attached
independently
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HRP20120738AT
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English (en)
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Robert Dean Dally
Sajan Joseph
Timothy Alan Shepherd
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Eli Lilly And Company
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Publication of HRP20120738T1 publication Critical patent/HRP20120738T1/hr

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • 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
    • A61P3/06Antihyperlipidemics
    • 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
    • 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
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D473/00Heterocyclic compounds containing purine ring systems
    • C07D473/26Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/32Nitrogen atom
    • C07D473/34Nitrogen atom attached in position 6, e.g. adenine

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Neurology (AREA)
  • Urology & Nephrology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Neurosurgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pulmonology (AREA)
  • Biomedical Technology (AREA)
  • Oncology (AREA)
  • Reproductive Health (AREA)
  • Emergency Medicine (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)

Claims (14)

1. Spoj formule: [image] naznačen time što: X je F, Cl, CF3, CN ili H; Y je F, H ili Cl; R1 i R2 su neovisno H, C1-C4 alkil ili CH2CH2OH; ili R1 i R2, zajedno s atomom dušika na kojeg su vezani, tvore pirolidinski prsten, izborno supstituiran s hidroksimetilom na položaju 2 ili s hidroksi na položaju 3, ili azetidinski prsten, supstituiran s hidroksi na položaju 3; R3 je H ili OH; R6 je H; ili R6 i R2, zajedno s atomom dušika na kojeg je R2 vezan, tvore piperidinski prsten; R7 i R8 su neovisno H ili CH3; ili R7 i R1, zajedno s atomom dušika na kojeg je R1 vezan, tvore pirolidinski prsten; W je CR4R5, NR10, C=O ili C=CH-R9; R4 i R5 su neovisno H, CH3 ili CH2CH3; R4 i R5, zajedno s atomom ugljika na kojeg su vezani, tvore ciklopentanski prsten; ili jedan od R4 ili R5 je benzil, a drugi je H; R9 je 2-tiazolil, 4-piridil, 2-metil-4-tiazolil, 2-imidazolil, 5-tiazolil ili 4-imidazolil; i R10 je H ili C1-C3 alkil; ili njegova farmaceutski prihvatljiva sol.
2. Spoj u skladu s patentnim zahtjevom 1, ili njegova farmaceutski prihvatljiva sol, naznačen time što Y je F.
3. Spoj u skladu s patentnim zahtjevom 1 ili claim 2, ili njegova farmaceutski prihvatljiva sol, naznačen time što X je Cl, CF3 ili F.
4. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 3, ili njegova farmaceutski prihvatljiva sol, naznačen time što W je CR4R5.
5. Spoj u skladu s patentnim zahtjevom 4, ili njegova farmaceutski prihvatljiva sol, naznačen time što su R4 i R5 neovisno H ili CH3, ili R4 i R5, zajedno s atomom ugljika na kojeg su vezani, tvore ciklopentanski prsten.
6. Spoju skladu s bilo kojim od patentnih zahtjeva 1 do 3, ili njegova farmaceutski prihvatljiva sol, naznačen time što W je NR10.
7. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 3, ili njegova farmaceutski prihvatljiva sol, naznačen time što W je C=CH-R9.
8. Spoj u skladu s patentnim zahtjevom 7, ili njegova farmaceutski prihvatljiva sol, naznačen time što R9 je 5-tiazolil.
9. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 8, ili njegova farmaceutski prihvatljiva sol, naznačen time što su R1 i R2 neovisno H, C1-C4 alkil ili CH2CH2OH; ili R1 i R2, zajedno s atomom dušika na kojeg su vezani, tvore pirolidinski prsten, izborno supstituiran s hidroksimetilom na položaju 2 ili s hidroksi na položaju 3.
10. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 9, ili njegova farmaceutski prihvatljiva sol, naznačen time što R3 je H.
11. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je 4-{4-[1-(2-dimetilaminoetil)-4-(4-fluor-3-trifluormetilphenil)-1H-imidazol-2-il]piperidin-1-il}-5,7-dihidropirolo[2,3-d]pirimidin-6-on, ili njegova farmaceutski prihvatljiva sol.
12. Farmaceutska formulacija, naznačena time što sadrži spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 11, ili njegovu farmaceutski prihvatljivu sol, kao i farmaceutski prihvatljivu podlogu, razrjeđivač ili pomoćnu tvar.
13. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 11, ili njegova farmaceutski prihvatljiva sol, naznačen time što je namijenjen upotrebi u terapiji.
14. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 11, ili njegova farmaceutski prihvatljiva sol, naznačen time što je namijenjen upotrebi u liječenju multiformnog glioblastoma.
HRP20120738AT 2008-11-11 2012-09-17 Inhibitori kinaza akt i p70 s6 HRP20120738T1 (hr)

Applications Claiming Priority (2)

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

Publications (1)

Publication Number Publication Date
HRP20120738T1 true HRP20120738T1 (hr) 2012-10-31

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Application Number Title Priority Date Filing Date
HRP20120738AT HRP20120738T1 (hr) 2008-11-11 2012-09-17 Inhibitori kinaza akt i p70 s6

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US (1) US8148387B2 (hr)
EP (1) EP2358710B1 (hr)
JP (1) JP5432275B2 (hr)
KR (1) KR101334460B1 (hr)
CN (1) CN102216302B (hr)
AR (1) AR074072A1 (hr)
AU (1) AU2009314324B2 (hr)
BR (1) BRPI0921916A2 (hr)
CA (1) CA2743019C (hr)
CO (1) CO6382114A2 (hr)
CR (1) CR20110240A (hr)
CY (1) CY1113409T1 (hr)
DK (1) DK2358710T3 (hr)
DO (1) DOP2011000129A (hr)
EA (1) EA018947B1 (hr)
EC (1) ECSP11011048A (hr)
ES (1) ES2391704T3 (hr)
HK (1) HK1158203A1 (hr)
HN (1) HN2011001247A (hr)
HR (1) HRP20120738T1 (hr)
IL (1) IL211940A (hr)
JO (1) JO2822B1 (hr)
MA (1) MA32776B1 (hr)
MX (1) MX2011005000A (hr)
MY (1) MY161461A (hr)
NZ (1) NZ592062A (hr)
PA (1) PA8846901A1 (hr)
PE (1) PE20110807A1 (hr)
PL (1) PL2358710T3 (hr)
PT (1) PT2358710E (hr)
RS (1) RS52520B (hr)
SI (1) SI2358710T1 (hr)
TN (1) TN2011000207A1 (hr)
TW (1) TWI422587B (hr)
UA (1) UA100190C2 (hr)
WO (1) WO2010056563A1 (hr)
ZA (1) ZA201102549B (hr)

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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
ES2646759T3 (es) 2011-09-12 2017-12-15 Merck Patent Gmbh Derivados de aminopirimidina para uso como moduladores de la actividad de la quinasa
DK2755965T3 (en) * 2011-09-12 2017-09-25 Merck Patent Gmbh PRESENT UNKNOWN IMIDAZOLAMINES AS MODULATORS OF KINASE ACTIVITY
AU2013344549B2 (en) 2012-11-16 2018-03-08 Xiaoling Chen Novel imidazol-piperidinyl derivatives as modulators of kinase activity
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
ES2746756T3 (es) * 2013-03-11 2020-03-06 Merck Patent Gmbh Derivados de 6-[4-(1H-imidazol-2-il)piperidin-1-il]pirimidin-4-amina como moduladores de la actividad cinasa
US9434714B2 (en) * 2014-02-11 2016-09-06 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
WO2017200087A1 (ja) * 2016-05-20 2017-11-23 大鵬薬品工業株式会社 新規5H-ピロロ[2,3-d]ピリミジン-6(7H)-オン誘導体
US20230148417A1 (en) * 2020-03-17 2023-05-11 Jiangsu Hengrui Pharmaceuticals Co., Ltd. Fused bicyclic derivative, preparation method therefor, and pharmaceutical use thereof
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

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UA99284C2 (ru) 2007-05-11 2012-08-10 Елі Ліллі Енд Компані ИНГИБИТОРЫ р70 S6-КИНАЗЫ

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SI2358710T1 (sl) 2012-11-30
EA201170680A1 (ru) 2011-12-30
AU2009314324A1 (en) 2010-05-20
ECSP11011048A (es) 2011-06-30
HN2011001247A (es) 2013-05-20
DOP2011000129A (es) 2016-02-29
TW201022268A (en) 2010-06-16
CA2743019C (en) 2013-08-13
PT2358710E (pt) 2012-10-01
WO2010056563A1 (en) 2010-05-20
RS52520B (en) 2013-04-30
NZ592062A (en) 2013-03-28
JP2012508274A (ja) 2012-04-05
PL2358710T3 (pl) 2012-12-31
CY1113409T1 (el) 2016-06-22
TWI422587B (zh) 2014-01-11
US8148387B2 (en) 2012-04-03
EP2358710A1 (en) 2011-08-24
DK2358710T3 (da) 2012-09-03
CA2743019A1 (en) 2010-05-20
EA018947B1 (ru) 2013-11-29
PE20110807A1 (es) 2011-10-31
BRPI0921916A2 (pt) 2015-12-29
CN102216302B (zh) 2013-08-21
MA32776B1 (fr) 2011-11-01
PA8846901A1 (es) 2010-06-28
JO2822B1 (en) 2014-09-15
IL211940A0 (en) 2011-06-30
HK1158203A1 (en) 2012-07-13
UA100190C2 (en) 2012-11-26
ES2391704T3 (es) 2012-11-29
KR101334460B1 (ko) 2013-12-02
CN102216302A (zh) 2011-10-12
EP2358710B1 (en) 2012-08-15
JP5432275B2 (ja) 2014-03-05
TN2011000207A1 (en) 2012-12-17
MY161461A (en) 2017-04-14
KR20110074578A (ko) 2011-06-30
ZA201102549B (en) 2012-09-26
AU2009314324B2 (en) 2013-06-20
AR074072A1 (es) 2010-12-22
MX2011005000A (es) 2011-05-25
IL211940A (en) 2014-01-30
CO6382114A2 (es) 2012-02-15
CR20110240A (es) 2011-06-09
US20100120801A1 (en) 2010-05-13

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