RU2012156958A - ПРОИЗВОДНЫЕ ТИЕНО[3,2-c]ПИРИДИНА В КАЧЕСТВЕ ИНГИБИТОРОВ КИНАЗ ДЛЯ ПРИМЕНЕНИЯ В ЛЕЧЕНИИ РАКА - Google Patents

ПРОИЗВОДНЫЕ ТИЕНО[3,2-c]ПИРИДИНА В КАЧЕСТВЕ ИНГИБИТОРОВ КИНАЗ ДЛЯ ПРИМЕНЕНИЯ В ЛЕЧЕНИИ РАКА Download PDF

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RU2012156958A
RU2012156958A RU2012156958/04A RU2012156958A RU2012156958A RU 2012156958 A RU2012156958 A RU 2012156958A RU 2012156958/04 A RU2012156958/04 A RU 2012156958/04A RU 2012156958 A RU2012156958 A RU 2012156958A RU 2012156958 A RU2012156958 A RU 2012156958A
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thieno
fluorophenyl
hydroxyethyl
urea
treatment
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RU2012156958/04A
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English (en)
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Майкл Р. МИКАЭЛИДЕС
Майкл Л. КЕРТИН
Робин Р. ФРЕЙ
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Эбботт Лэборетриз
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Publication of RU2012156958A publication Critical patent/RU2012156958A/ru

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—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
    • A61K31/435—Heterocyclic 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
    • A61K31/4353—Heterocyclic 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
    • A61K31/4365—Heterocyclic 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 the heterocyclic ring system having sulfur as a ring hetero atom, e.g. ticlopidine
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D333/30—Hetero atoms other than halogen
    • C07D333/36—Nitrogen atoms

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Enzymes And Modification Thereof (AREA)

Abstract

1. N-(4-{4-амино-7-[1-(2-гидроксиэтил)-1Н-пиразол-4-ил]тиено[3,2-с]пиридин-3-ил}фенил-N'-(3-фторфенил)мочевину или его терапевтически приемлемую соль для применения в лечении острого миелолейкоза.2. Комбинация (а) N-(4-{4-амино-7-[1-(2-гидроксиэтил)-1Н-пиразол-4-ил]тиено[3,2-с]пиридин-3-ил}фенил-N'-(3-фторфенил)мочевину или его терапевтически приемлемой соли и (b) 5-азацитидина для применения в лечении острого миелолейкоза.3. N-(4-{4-амино-7-[1-(2-гидроксиэтил)-1Н-пиразол-4-ил]тиено[3,2-с]пиридин-3-ил}фенил-N'-(3-фторфенил)мочевину или его терапевтически приемлемую соль для применения в лечении немелкоклеточного рака легких.4. Комбинация (а) N-(4-{4-амино-7-[1-(2-гидроксиэтил)-1Н-пиразол-4-ил]тиено[3,2-с]пиридин-3-ил}фенил-N'-(3-фторфенил)мочевину или его терапевтически приемлемой соли и (b) доцетаксела для применения в лечении немелкоклеточного рака легких.5. N-(4-{4-амино-7-[1-(2-гидроксиэтил)-1Н-пиразол-4-ил]тиено[3,2-с]пиридин-3-ил}фенил-N'-(3-фторфенил)мочевину или его терапевтически приемлемую соль для применения в лечении рака толстой кишки.6. N-(4-{4-амино-7-[1-(2-гидроксиэтил)-1Н-пиразол-4-ил]тиено[3,2-с]пиридин-3-ил}фенил-N'-(3-фторфенил)мочевину или его терапевтически приемлемую соль для применения в лечении рака яичников.7. Комбинация (а) N-(4-{4-амино-7-[1-(2-гидроксиэтил)-1Н-пиразол-4-ил]тиено[3,2-с]пиридин-3-ил}фенил-N'-(3-фторфенил)мочевину или его терапевтически приемлемой соли и (b) цисплатина для применения в лечении рака яичников.

Claims (7)

1. N-(4-{4-амино-7-[1-(2-гидроксиэтил)-1Н-пиразол-4-ил]тиено[3,2-с]пиридин-3-ил}фенил-N'-(3-фторфенил)мочевину или его терапевтически приемлемую соль для применения в лечении острого миелолейкоза.
2. Комбинация (а) N-(4-{4-амино-7-[1-(2-гидроксиэтил)-1Н-пиразол-4-ил]тиено[3,2-с]пиридин-3-ил}фенил-N'-(3-фторфенил)мочевину или его терапевтически приемлемой соли и (b) 5-азацитидина для применения в лечении острого миелолейкоза.
3. N-(4-{4-амино-7-[1-(2-гидроксиэтил)-1Н-пиразол-4-ил]тиено[3,2-с]пиридин-3-ил}фенил-N'-(3-фторфенил)мочевину или его терапевтически приемлемую соль для применения в лечении немелкоклеточного рака легких.
4. Комбинация (а) N-(4-{4-амино-7-[1-(2-гидроксиэтил)-1Н-пиразол-4-ил]тиено[3,2-с]пиридин-3-ил}фенил-N'-(3-фторфенил)мочевину или его терапевтически приемлемой соли и (b) доцетаксела для применения в лечении немелкоклеточного рака легких.
5. N-(4-{4-амино-7-[1-(2-гидроксиэтил)-1Н-пиразол-4-ил]тиено[3,2-с]пиридин-3-ил}фенил-N'-(3-фторфенил)мочевину или его терапевтически приемлемую соль для применения в лечении рака толстой кишки.
6. N-(4-{4-амино-7-[1-(2-гидроксиэтил)-1Н-пиразол-4-ил]тиено[3,2-с]пиридин-3-ил}фенил-N'-(3-фторфенил)мочевину или его терапевтически приемлемую соль для применения в лечении рака яичников.
7. Комбинация (а) N-(4-{4-амино-7-[1-(2-гидроксиэтил)-1Н-пиразол-4-ил]тиено[3,2-с]пиридин-3-ил}фенил-N'-(3-фторфенил)мочевину или его терапевтически приемлемой соли и (b) цисплатина для применения в лечении рака яичников.
RU2012156958/04A 2008-12-05 2012-12-25 ПРОИЗВОДНЫЕ ТИЕНО[3,2-c]ПИРИДИНА В КАЧЕСТВЕ ИНГИБИТОРОВ КИНАЗ ДЛЯ ПРИМЕНЕНИЯ В ЛЕЧЕНИИ РАКА RU2012156958A (ru)

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US12028108P 2008-12-05 2008-12-05
US61/120,281 2008-12-05
US22376009P 2009-07-08 2009-07-08
US61/223,760 2009-07-08

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RU2011127451A (ru) 2013-01-10
UA103351C2 (ru) 2013-10-10
AR074481A1 (es) 2011-01-19
WO2010065825A2 (en) 2010-06-10
HK1159628A1 (en) 2012-08-03
JP5588458B2 (ja) 2014-09-10
PE20110830A1 (es) 2011-12-14
PA8852401A1 (es) 2010-07-27
AU2009322270A1 (en) 2011-07-14
KR20110091577A (ko) 2011-08-11
MX2011005943A (es) 2011-06-27
RU2480472C2 (ru) 2013-04-27
DOP2011000153A (es) 2011-06-30
TWI441827B (zh) 2014-06-21
AU2009322270B2 (en) 2014-12-18
ECSP11011172A (es) 2011-08-31
IL212716A0 (en) 2011-07-31
EP2373662A2 (en) 2011-10-12
US20100144783A1 (en) 2010-06-10
MY179042A (en) 2020-10-26
CO6382131A2 (es) 2012-02-15
WO2010065825A3 (en) 2010-08-26
UY32291A (es) 2010-07-30
JP2012511016A (ja) 2012-05-17
CA2743592A1 (en) 2010-06-10
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US8722890B2 (en) 2014-05-13
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IL212716A (en) 2013-10-31
TWI500621B (zh) 2015-09-21
US20120309783A1 (en) 2012-12-06
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BRPI0921392A2 (pt) 2016-04-26

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