CY1118112T1 - Διυποκατεστημενες βενζοθειενυλ-πυρρολοτριαζινες και η χρηση τους ως αναστολεις κινασης υποδοχεα του αυξητικου παραγοντα των ινοβλαστων (fgfr) - Google Patents

Διυποκατεστημενες βενζοθειενυλ-πυρρολοτριαζινες και η χρηση τους ως αναστολεις κινασης υποδοχεα του αυξητικου παραγοντα των ινοβλαστων (fgfr)

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Publication number
CY1118112T1
CY1118112T1 CY20161100853T CY161100853T CY1118112T1 CY 1118112 T1 CY1118112 T1 CY 1118112T1 CY 20161100853 T CY20161100853 T CY 20161100853T CY 161100853 T CY161100853 T CY 161100853T CY 1118112 T1 CY1118112 T1 CY 1118112T1
Authority
CY
Cyprus
Prior art keywords
hydrogen
compounds
differentialized
benzothythenyl
pyrrolotriazines
Prior art date
Application number
CY20161100853T
Other languages
English (en)
Inventor
Dirk Brohm
Melanie Heroult
Marie-Pierre Collin
Walter Hübsch
Mario Lobell
Klemens Lustig
Sylvia Grünewald
Ulf Bömer
Verena VÖHRINGER
Original Assignee
Bayer Pharma Aktiengesellschaft
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 Bayer Pharma Aktiengesellschaft filed Critical Bayer Pharma Aktiengesellschaft
Publication of CY1118112T1 publication Critical patent/CY1118112T1/el

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Classifications

    • 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
    • A61K31/53Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • 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
    • A61K31/5355Non-condensed oxazines and containing further heterocyclic rings
    • 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
    • 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
    • A61K31/54Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541Non-condensed thiazines containing further heterocyclic rings
    • 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
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur 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
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings

Abstract

Αυτή η εφεύρεση αναφέρεται σε νέα υποκατεστημένο παράγωγο της 5-(1-βενζοθειοφαιν-2-υλο) πυρρολο[2,1-f][1,2,4]τριαζιν-4-αμίνης του τύπου (I) όπου το R1 είναι υδρογόνο, χλώριο, μεθύλιο ή μεθοξύ, το R2 είναι υδρογόνο ή μεθοξύ, με την προϋπόθεση ότι τουλάχιστον ένα εκ των R1 και R2 είναι άλλο εκτός από υδρογόνο, το G1 είναι χλώριο, (C1-C4)-αλκύλιο, (C1-C4)-αλκοξυκαρβονυλιο, 5-μελές αζα-ετεροαρύλιο, ή η ομάδα -CH2-OR3, -CH2-NR4R5 ή -C(=0)- NR4R6, και το G2 είναι χλώριο, κυάνιο, (C1-C4)-αλκύλιο ή η ομάδα - CR8AR8B-OH, -CH2-NR9R10, -C(=0)-NR11R12 ή -CH2-OR15, που έχουν ανασταλτικές δράσεις της πρωτεϊνικής κινάσης τυροσίνης, σε διαδικασίες για την παρασκευή τέτοιων ενώσεων, σε φαρμακευτικές συνθέσεις που περιέχουν τέτοιες ενώσεις, και στη χρήση τέτοιων ενώσεων ή συνθέσεων για την θεραπεία νεοπλαστικών διαταραχών, ιδιαίτερα των παθήσεων καρκίνου και όγκου.
CY20161100853T 2011-12-15 2016-08-31 Διυποκατεστημενες βενζοθειενυλ-πυρρολοτριαζινες και η χρηση τους ως αναστολεις κινασης υποδοχεα του αυξητικου παραγοντα των ινοβλαστων (fgfr) CY1118112T1 (el)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP11193841 2011-12-15
EP12798738.6A EP2791140B1 (en) 2011-12-15 2012-12-10 Disubstituted benzothienyl-pyrrolotriazines and their use as fgfr kinase inhibitors
PCT/EP2012/074977 WO2013087578A1 (en) 2011-12-15 2012-12-10 Disubstituted benzothienyl-pyrrolotriazines and their use as fgfr kinase inhibitors

Publications (1)

Publication Number Publication Date
CY1118112T1 true CY1118112T1 (el) 2017-06-28

Family

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CY20161100853T CY1118112T1 (el) 2011-12-15 2016-08-31 Διυποκατεστημενες βενζοθειενυλ-πυρρολοτριαζινες και η χρηση τους ως αναστολεις κινασης υποδοχεα του αυξητικου παραγοντα των ινοβλαστων (fgfr)

Country Status (43)

Country Link
US (4) US20140336173A1 (el)
EP (1) EP2791140B1 (el)
JP (1) JP6050829B2 (el)
KR (1) KR102057444B1 (el)
CN (1) CN104245700B (el)
AR (1) AR089207A1 (el)
AU (3) AU2012350750B2 (el)
BR (1) BR112014014531B1 (el)
CA (1) CA2859133C (el)
CL (1) CL2014001547A1 (el)
CO (1) CO7030961A2 (el)
CR (1) CR20140288A (el)
CU (2) CU24426B1 (el)
CY (1) CY1118112T1 (el)
DK (1) DK2791140T3 (el)
DO (1) DOP2014000127A (el)
EA (1) EA029556B1 (el)
EC (1) ECSP14004722A (el)
ES (1) ES2591203T3 (el)
GT (1) GT201400113A (el)
HK (1) HK1205123A1 (el)
HR (1) HRP20161130T1 (el)
HU (1) HUE029582T2 (el)
IL (1) IL232611A (el)
IN (1) IN2014CN04310A (el)
JO (1) JO3295B1 (el)
LT (1) LT2791140T (el)
ME (1) ME02517B (el)
MX (1) MX367158B (el)
MY (1) MY178660A (el)
PE (1) PE20141855A1 (el)
PH (1) PH12014501355A1 (el)
PL (1) PL2791140T3 (el)
PT (1) PT2791140T (el)
RS (1) RS55144B1 (el)
SG (1) SG11201402325QA (el)
SI (1) SI2791140T1 (el)
TN (1) TN2014000255A1 (el)
TW (1) TWI567076B (el)
UA (1) UA116768C2 (el)
UY (1) UY34484A (el)
WO (1) WO2013087578A1 (el)
ZA (1) ZA201405140B (el)

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US9206184B2 (en) 2015-12-08
AR089207A1 (es) 2014-08-06
ME02517B (me) 2017-02-20
MY178660A (en) 2020-10-20
CA2859133A1 (en) 2013-06-20
CU24426B1 (es) 2019-06-04
DK2791140T3 (en) 2016-09-19
LT2791140T (lt) 2016-10-10
JP6050829B2 (ja) 2016-12-21
TW201339162A (zh) 2013-10-01
PH12014501355B1 (en) 2014-09-22
KR20140103328A (ko) 2014-08-26
CU20160039A7 (es) 2016-08-31
PT2791140T (pt) 2016-09-20
US20220153745A1 (en) 2022-05-19
DOP2014000127A (es) 2014-08-15
EA029556B1 (ru) 2018-04-30
RS55144B1 (sr) 2016-12-30
EP2791140A1 (en) 2014-10-22
IL232611A (en) 2017-05-29
TN2014000255A1 (en) 2015-09-30
TWI567076B (zh) 2017-01-21
AU2017206140A1 (en) 2017-08-03
JO3295B1 (ar) 2018-09-16
NZ625073A (en) 2016-07-29
GT201400113A (es) 2015-08-25
JP2015500307A (ja) 2015-01-05
US20140336173A1 (en) 2014-11-13
HRP20161130T1 (hr) 2016-11-18
CN104245700A (zh) 2014-12-24
SG11201402325QA (en) 2014-09-26
IN2014CN04310A (el) 2015-09-04
CA2859133C (en) 2020-03-24
HK1205123A1 (en) 2015-12-11
CU20140065A7 (es) 2014-11-27
ZA201405140B (en) 2017-04-26
MX2014006905A (es) 2014-09-08
PL2791140T3 (pl) 2017-08-31
IL232611A0 (en) 2014-06-30
AU2019204255A1 (en) 2019-07-04
US20130158000A1 (en) 2013-06-20
ECSP14004722A (es) 2015-11-30
BR112014014531B1 (pt) 2022-02-08
US20190016724A1 (en) 2019-01-17
AU2012350750A1 (en) 2014-06-12
EA201400707A1 (ru) 2014-11-28
BR112014014531A2 (pt) 2019-08-06
KR102057444B1 (ko) 2019-12-19
UA116768C2 (uk) 2018-05-10
CO7030961A2 (es) 2014-08-21
EP2791140B1 (en) 2016-06-15
UY34484A (es) 2013-07-31
CL2014001547A1 (es) 2014-10-24
PH12014501355A1 (en) 2014-09-22
CR20140288A (es) 2014-07-14
ES2591203T3 (es) 2016-11-25
CN104245700B (zh) 2016-11-16
AU2012350750B2 (en) 2017-08-03
SI2791140T1 (sl) 2016-10-28
HUE029582T2 (en) 2017-03-28
PE20141855A1 (es) 2014-11-26
MX367158B (es) 2019-08-07
WO2013087578A1 (en) 2013-06-20

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