SI3124025T1 - Kombinacija med 3-((3-((4-(4-morfolinilmetil)-1h-pirol-2-il)metilen)-2- okso-2,3-dihidro-1h-indol-5-il)metil)-1,3-tiazolidin-2,4-dionom in inhibitorjem tirozin kinaze egfr - Google Patents

Kombinacija med 3-((3-((4-(4-morfolinilmetil)-1h-pirol-2-il)metilen)-2- okso-2,3-dihidro-1h-indol-5-il)metil)-1,3-tiazolidin-2,4-dionom in inhibitorjem tirozin kinaze egfr Download PDF

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Publication number
SI3124025T1
SI3124025T1 SI201630028T SI201630028T SI3124025T1 SI 3124025 T1 SI3124025 T1 SI 3124025T1 SI 201630028 T SI201630028 T SI 201630028T SI 201630028 T SI201630028 T SI 201630028T SI 3124025 T1 SI3124025 T1 SI 3124025T1
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SI
Slovenia
Prior art keywords
morpholinylmethyl
pyrrol
indol
dihydro
oxo
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SI201630028T
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English (en)
Inventor
Michael Frank Burbridge
Valerie Cattan
Anne Jacquet-Bescond
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Les Laboratoires Servier
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Application filed by Les Laboratoires Servier filed Critical Les Laboratoires Servier
Publication of SI3124025T1 publication Critical patent/SI3124025T1/sl

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/14—Heterocyclic 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
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/426—1,3-Thiazoles
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
    • 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
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • A61K31/535—Heterocyclic 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
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • 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
    • A61P35/00—Antineoplastic agents
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic 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
    • 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
    • A61K31/47—Quinolines; Isoquinolines

Claims (10)

  1. KOMBINACIJA MED 3-[(3-{[4-(4-MORFOLINILMETIL)-1H-PIROL-2-IL]METILEN}-2-OKSO-2,3-DIHIDRO-1H-INDOL-5-IL)METIL]-1,3-TIAZOLIDIN-2,4-DIONOM IN INHIBITORJEM TIROZIN KINAZE EGFR Patentni zahtevki
    1. Kombinacija med 3-[(3-{[4-(4-morfolinilmetil)-1/-/-pirol-2-il]metilen}-2-okso-2,3-dihidro-1 H-indol-5-il)metil]-1,3-tiazolidin-2,4-dionom s formulo (I):
    ter njegovimi Z ali E izomeri in/ali dodatnimi solmi s farmacevtsko sprejemljivo kislino ali bazo in inhibitorjem tirozin kinaze receptorja za humani epidermalni rastni faktor (EGFR).
  2. 2. Kombinacija po zahtevku 1, označena s tem, da se 3-[(3-{[4-(4-morfolinilmetil)-1 H-pirol-2-il]metilen}-2-okso-2,3-dihidro-1 H-indol-5-il)metil]-1,3-tiazolidin-2,4-dion uporablja v obliki Z izomera.
  3. 3. Kombinacija po katerem koli izmed zahtevkov 1 ali 2, označena s tem, da se 3-[(3-{[4-(4-morfolinilmetil)-1H-pirol-2-il]metilen}-2-okso-2,3-dihidro-1/-/-indol-5-il)metil]-1,3-tiazolidin-2,4-dion uporablja v obliki hidroklorida.
  4. 4. Kombinacija po katerem koli izmed zahtevkov 1 ali 2, označena s tem, da se 3-[(3-{[4-(4-morfolinilmetil)-1/-/-pirol-2-il]metilen}-2-okso-2,3-dihidro-1/-/-indol-5-il)metil]-1,3-tiazolidin-2,4-dion uporablja v obliki mesilata.
  5. 5. Kombinacija po katerem koli izmed zahtevkov od 1 dtf VdznačBiraVtem’'daje inhibitor tirozin kinaze EGFR gefitinib ali erlotinib.
  6. 6. Kombinacija po katerem koli izmed zahtevkov od 1 do 5 za uporabo pri zdravljenju nedrobnoceličnega raka pljuč.
  7. 7. Kombinacija po katerem koli izmed zahtevkov od 1 do 5 za uporabo pri zdravljenju nedrobnoceličnega raka pljuč pri bolnikih, ki so odporni na inhibitor tirozin kinaze EGFR.
  8. 8. Farmacevtski sestavek, ki kot zdravilno učinkovino/aktivno sestavino obsega 3-[(3-{[4-(4-morfolinilmetil)-1H-pirol-2-il]metilen}-2-okso-2,3-dihidro-1H-indol-5-il)metil]-1,3-tiazolidin-2,4-dion oziroma njegov Z ali E izomer in/ali njegove dodatne soli s farmacevtsko sprejemljivo kislino ali bazo v kombinaciji z inhibitorjem tirozin kinaze EGFR, po katerem koli izmed zahtevkov od 1 do 7 v kombinaciji z eno ali več farmacevtsko sprejemljivimi pomožnimi snovmi.
  9. 9. Farmacevtski sestavek po zahtevku 8 za uporabo pri zdravljenju nedrobnoceličnega raka pljuč.
  10. 10. Farmacevtski sestavek po zahtevku 9 za uporabo pri zdravljenju nedrobnoceličnega raka pljuč pri bolnikih, ki so odporni na inhibitor tirozin kinaze EGFR.
SI201630028T 2015-07-31 2016-07-29 Kombinacija med 3-((3-((4-(4-morfolinilmetil)-1h-pirol-2-il)metilen)-2- okso-2,3-dihidro-1h-indol-5-il)metil)-1,3-tiazolidin-2,4-dionom in inhibitorjem tirozin kinaze egfr SI3124025T1 (sl)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
FR1557412A FR3039401B1 (fr) 2015-07-31 2015-07-31 Nouvelle association entre le 3-[(3-{[4-(4-morpholinylmethyl)-1h-pyrrol-2-yl]methylene}-2-oxo-2,3-dihydro-1h-indol-5-yl)methyl]-1,3-thiazolidine-2,4-dione et un inhibiteur de la tyr kinase du egfr
EP16181821.6A EP3124025B1 (fr) 2015-07-31 2016-07-29 Association entre le 3-[(3-{[4-(4-morpholinylméthyl)-1h-pyrrol-2-yl]méthylène}-2-oxo-2,3-dihydro-1h-indol-5-yl)méthyl]-1,3-thiazolidine-2,4-dione et un inhibiteur de la tyr kinase du egfr

Publications (1)

Publication Number Publication Date
SI3124025T1 true SI3124025T1 (sl) 2018-04-30

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ID=55299545

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SI201630028T SI3124025T1 (sl) 2015-07-31 2016-07-29 Kombinacija med 3-((3-((4-(4-morfolinilmetil)-1h-pirol-2-il)metilen)-2- okso-2,3-dihidro-1h-indol-5-il)metil)-1,3-tiazolidin-2,4-dionom in inhibitorjem tirozin kinaze egfr

Country Status (40)

Country Link
US (1) US20170027952A1 (sl)
EP (1) EP3124025B1 (sl)
JP (2) JP2017061445A (sl)
KR (1) KR101822492B1 (sl)
CN (1) CN106397427A (sl)
AR (1) AR105527A1 (sl)
AU (1) AU2016206300A1 (sl)
BR (1) BR102016017404A2 (sl)
CA (1) CA2936904C (sl)
CL (1) CL2018000256A1 (sl)
CO (1) CO2018000953A2 (sl)
CR (1) CR20180044A (sl)
CU (1) CU20180013A7 (sl)
CY (1) CY1120792T1 (sl)
DK (1) DK3124025T3 (sl)
EA (1) EA032217B1 (sl)
EC (1) ECSP18003671A (sl)
ES (1) ES2671133T3 (sl)
FR (1) FR3039401B1 (sl)
HR (1) HRP20180760T1 (sl)
HU (1) HUE037632T2 (sl)
IL (1) IL257232A (sl)
LT (1) LT3124025T (sl)
MA (1) MA39693B1 (sl)
MD (1) MD3124025T2 (sl)
ME (1) ME03052B (sl)
MX (1) MX366748B (sl)
NO (1) NO3124025T3 (sl)
PE (1) PE20190350A1 (sl)
PH (1) PH12016000248A1 (sl)
PL (1) PL3124025T3 (sl)
PT (1) PT3124025T (sl)
RS (1) RS57057B1 (sl)
RU (1) RU2695362C2 (sl)
SG (1) SG10201605664SA (sl)
SI (1) SI3124025T1 (sl)
SV (1) SV2018005615A (sl)
TN (1) TN2018000028A1 (sl)
TW (1) TWI623315B (sl)
WO (1) WO2017021634A1 (sl)

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KR101956978B1 (ko) * 2015-05-18 2019-03-12 주식회사 케이티 시스템 정보 송수신 방법 및 그 장치

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* Cited by examiner, † Cited by third party
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SI2068880T1 (sl) * 2006-09-18 2012-08-31 Boehringer Ingelheim Int Postopek za zdravljenje raka, ki vsebuje mutacije EGFR
CA2678043A1 (en) * 2007-03-01 2008-09-04 Novartis Ag Acid addition salts, hydrates and polymorphs of 5-(2,4-dihydroxy-5-isopropyl-phenyl)-4-(4-morpholin-4-ylmethyl-phenyl)-isoxazole-3-carboxylic acid ethylamide and formulations comprising these forms
JPWO2008108386A1 (ja) * 2007-03-05 2010-06-17 協和発酵キリン株式会社 医薬組成物
UY31800A (es) * 2008-05-05 2009-11-10 Smithkline Beckman Corp Metodo de tratamiento de cancer usando un inhibidor de cmet y axl y un inhibidor de erbb
FR2948940B1 (fr) * 2009-08-04 2011-07-22 Servier Lab Nouveaux derives dihydroindolones, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
JP5945863B2 (ja) * 2012-01-06 2016-07-05 国立大学法人高知大学 腎細胞がん治療剤
CA2902263A1 (en) * 2013-03-06 2014-09-12 Genentech, Inc. Methods of treating and preventing cancer drug resistance
FR3008411B1 (fr) * 2013-07-12 2015-07-03 Servier Lab Nouveau sel de la 3-[(3-{[4-(4-morpholinylmethyl)-1h-pyrrol-2-yl]methylene}-2-oxo-2,3-dihydro-1h-indol-5-yl)methyl]-1,3-thiazolidine-2,4-dione, sa preparation, et les formulations qui le contiennent
RU2016132400A (ru) * 2014-01-07 2018-02-13 Мерк Патент Гмбх Комбинация производного 6-оксо-1,6-дигидро-пиридазина, имеющего противораковую активность, с гефитинибом
US20170304313A1 (en) * 2014-10-06 2017-10-26 Novartis Ag Therapeutic Combination For The Treatment Of Cancer

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Publication number Publication date
HRP20180760T1 (hr) 2018-06-15
US20170027952A1 (en) 2017-02-02
HUE037632T2 (hu) 2018-09-28
MA39693A (fr) 2017-02-01
PL3124025T3 (pl) 2018-06-29
MX2016009743A (es) 2017-03-03
EP3124025A1 (fr) 2017-02-01
FR3039401B1 (fr) 2018-07-13
ME03052B (me) 2018-10-20
NO3124025T3 (sl) 2018-07-28
TW201711686A (zh) 2017-04-01
CA2936904A1 (fr) 2017-01-31
EA201600507A3 (ru) 2017-03-31
CY1120792T1 (el) 2019-12-11
ES2671133T3 (es) 2018-06-05
CN106397427A (zh) 2017-02-15
PE20190350A1 (es) 2019-03-07
SV2018005615A (es) 2018-05-14
CA2936904C (fr) 2018-12-04
ECSP18003671A (es) 2018-03-31
AU2016206300A1 (en) 2017-02-16
DK3124025T3 (en) 2018-06-06
MX366748B (es) 2019-07-23
KR20170015218A (ko) 2017-02-08
JP2017061445A (ja) 2017-03-30
EP3124025B1 (fr) 2018-02-28
IL257232A (en) 2018-03-29
WO2017021634A1 (fr) 2017-02-09
FR3039401A1 (fr) 2017-02-03
TN2018000028A1 (fr) 2019-07-08
EA201600507A2 (ru) 2017-02-28
KR101822492B1 (ko) 2018-01-29
PH12016000248A1 (en) 2018-01-22
CL2018000256A1 (es) 2018-04-06
MD3124025T2 (ro) 2018-06-30
TWI623315B (zh) 2018-05-11
SG10201605664SA (en) 2017-02-27
CR20180044A (es) 2018-04-03
EA032217B1 (ru) 2019-04-30
BR102016017404A2 (pt) 2017-02-07
RS57057B1 (sr) 2018-05-31
CU20180013A7 (es) 2018-05-08
JP2019163306A (ja) 2019-09-26
PT3124025T (pt) 2018-04-09
MA39693B1 (fr) 2018-07-31
AR105527A1 (es) 2017-10-11
CO2018000953A2 (es) 2018-07-10
RU2016131395A3 (sl) 2018-06-08
RU2016131395A (ru) 2018-02-02
LT3124025T (lt) 2018-03-26
RU2695362C2 (ru) 2019-07-23

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