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PE20130149A1 - Derivados de la cromenona con actividad anti-tumoral - Google Patents

Derivados de la cromenona con actividad anti-tumoral

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Publication number
PE20130149A1
PE20130149A1 PE2012000578A PE2012000578A PE20130149A1 PE 20130149 A1 PE20130149 A1 PE 20130149A1 PE 2012000578 A PE2012000578 A PE 2012000578A PE 2012000578 A PE2012000578 A PE 2012000578A PE 20130149 A1 PE20130149 A1 PE 20130149A1
Authority
PE
Peru
Prior art keywords
ethyl
alkyl
halogen
chromenone
alcoxy
Prior art date
Application number
PE2012000578A
Other languages
English (en)
Inventor
Bernard Christophe Barlaam
Sebastien Louis Degorce
Der Brempt Christine Marie Paul Lambert-Van
Remy Robert Morgentin
Patrick Ple
Original Assignee
Astrazeneca Ab
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Astrazeneca Ab filed Critical Astrazeneca Ab
Publication of PE20130149A1 publication Critical patent/PE20130149A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D311/00Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
    • C07D311/02Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D311/74Benzo[b]pyrans, hydrogenated in the carbocyclic ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D311/00Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
    • C07D311/02Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D311/04Benzo[b]pyrans, not hydrogenated in the carbocyclic ring
    • C07D311/22Benzo[b]pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 4
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/275Nitriles; Isonitriles
    • A61K31/277Nitriles; Isonitriles having a ring, e.g. verapamil
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/337Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
    • 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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02Silicon compounds
    • C07F7/08Compounds having one or more C—Si linkages
    • C07F7/18Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
    • C07F7/1804Compounds having Si-O-C linkages
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07Optical isomers

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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)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyrane Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

SE REFIERE A COMPUESTOS DERIVADOS DE CROMENONA DE FORMULA (I) DONDE R1 ES H O ALQUILO(C1-C4) OPCIONALMENTE SUSTITUIDO CON HALOGENO, HIDROXI O ALCOXI(C1-C3); R2 ES ALQUILO(C1-C4) O ALCOXI(C1-C4) OPCIONALMENTE SUSTITUIDO CON HALOGENO, HIDROXI, ALQUENILO(C2-C3), ENTRE OTROS; R3 ES H O ALQUILO(C1-C3); R4 Y R5 SON CADA UNO H, HALOGENO, ALQUILO(C1-C3), ALQUENILO(C2-C3), CN, ENTRE OTROS; R6, R7 Y R8 SON CADA UNO H, HALOGENO, ALQUILO(C1-C3), ALCOXI(C1-C3), ENTRE OTROS; R9 ES ALQUILO(C1-C3); n ES DE 0 A 4. SON COMPUESTOS PREFERIDOS: N-(2-(DIMETILAMINO)ETIL)-8-(1-(4-FLUOROFENILAMINO)ETIL)-2-MORFOLINO-4-OXO-4H-CROMENO-6-CARBOXAMIDA; N-(2-(DIMETILAMINO)ETIL)-2-MORFOLINO-4-OXO-8-(1-(FENILAMINO)ETIL)-4H-CROMENO-6-CARBOXAMIDA; 8-(1-(3-CLORO-2-FLUOROFENILAMINO)ETIL)-N-(2-(DIMETILAMINO)ETIL)-2-MORFOLINO-4-OXO-4H-CROMENO-6-CARBOXAMIDA; ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE FOSFOINOSITIDA (PI) 3-QUINASA ? SIENDO UTILES EN EL TRATAMIENTO DE CANCER
PE2012000578A 2009-10-27 2010-10-25 Derivados de la cromenona con actividad anti-tumoral PE20130149A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP09306017 2009-10-27

Publications (1)

Publication Number Publication Date
PE20130149A1 true PE20130149A1 (es) 2013-03-10

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PE2012000578A PE20130149A1 (es) 2009-10-27 2010-10-25 Derivados de la cromenona con actividad anti-tumoral

Country Status (42)

Country Link
US (5) US8399460B2 (es)
EP (1) EP2493870B1 (es)
JP (2) JP5657010B2 (es)
KR (1) KR101738195B1 (es)
CN (2) CN102712615B (es)
AR (1) AR078786A1 (es)
AU (1) AU2010311107B9 (es)
BR (1) BR112012010124B8 (es)
CA (1) CA2776994C (es)
CL (1) CL2012001056A1 (es)
CO (1) CO6541528A2 (es)
CR (1) CR20120217A (es)
CU (1) CU20120069A7 (es)
CY (1) CY1116143T1 (es)
DK (1) DK2493870T3 (es)
DO (1) DOP2012000124A (es)
EA (1) EA020523B9 (es)
EC (1) ECSP12011838A (es)
ES (1) ES2530943T3 (es)
GT (1) GT201200126A (es)
HK (2) HK1174027A1 (es)
HN (1) HN2012000889A (es)
HR (1) HRP20150146T1 (es)
IL (1) IL219191A0 (es)
IN (1) IN2012DN03328A (es)
ME (1) ME02050B (es)
MX (1) MX2012005027A (es)
MY (1) MY179833A (es)
NI (1) NI201200081A (es)
NZ (1) NZ599457A (es)
PE (1) PE20130149A1 (es)
PH (1) PH12012500804A1 (es)
PL (1) PL2493870T3 (es)
PT (1) PT2493870E (es)
RS (1) RS53813B1 (es)
SA (1) SA110310808B1 (es)
SI (1) SI2493870T1 (es)
SM (1) SMT201500036B (es)
TW (1) TWI483939B (es)
UA (1) UA107474C2 (es)
UY (1) UY32978A (es)
WO (1) WO2011051704A1 (es)

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US9029374B2 (en) 2015-05-12
EA201200618A1 (ru) 2012-12-28
CN104447657B (zh) 2016-08-17
UA107474C2 (uk) 2015-01-12
JP2013508449A (ja) 2013-03-07
UY32978A (es) 2011-05-31
US8673906B2 (en) 2014-03-18
IL219191A0 (en) 2012-06-28
GT201200126A (es) 2014-03-03
WO2011051704A1 (en) 2011-05-05
SMT201500036B (it) 2015-05-05
US9718800B2 (en) 2017-08-01
IN2012DN03328A (es) 2015-10-23
CN102712615A (zh) 2012-10-03
CO6541528A2 (es) 2012-10-16
CN104447657A (zh) 2015-03-25
EP2493870A1 (en) 2012-09-05
CA2776994A1 (en) 2011-05-05
US20110098271A1 (en) 2011-04-28
HN2012000889A (es) 2015-08-03
HRP20150146T1 (hr) 2015-05-22
CN102712615B (zh) 2014-12-17
KR101738195B1 (ko) 2017-05-19
ME02050B (me) 2015-05-20
JP5657010B2 (ja) 2015-01-21
PL2493870T3 (pl) 2015-04-30
BR112012010124B1 (pt) 2021-02-17
AU2010311107B9 (en) 2014-06-19
PT2493870E (pt) 2015-02-18
TWI483939B (zh) 2015-05-11
US20130158026A1 (en) 2013-06-20
US20160272607A1 (en) 2016-09-22
NZ599457A (en) 2014-04-30
PH12012500804A1 (en) 2022-10-03
HK1206335A1 (zh) 2016-01-08
JP2015078202A (ja) 2015-04-23
DK2493870T3 (en) 2015-02-23
CU20120069A7 (es) 2012-10-15
ES2530943T3 (es) 2015-03-09
JP5872016B2 (ja) 2016-03-01
CL2012001056A1 (es) 2012-10-05
SI2493870T1 (sl) 2015-03-31
AU2010311107B2 (en) 2014-03-27
EA020523B1 (ru) 2014-11-28
US20140194419A1 (en) 2014-07-10
AR078786A1 (es) 2011-11-30
MY179833A (en) 2020-11-17
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US20160060240A1 (en) 2016-03-03
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US8399460B2 (en) 2013-03-19
TW201121960A (en) 2011-07-01
ECSP12011838A (es) 2012-06-29
EA020523B9 (ru) 2015-01-30
CY1116143T1 (el) 2017-02-08
NI201200081A (es) 2012-11-07
EP2493870B1 (en) 2014-12-17
MX2012005027A (es) 2012-09-07
KR20120098724A (ko) 2012-09-05
RS53813B1 (en) 2015-06-30
BR112012010124A2 (pt) 2016-06-07
AU2010311107A1 (en) 2012-05-03

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