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PE20130386A1 - Derivados de indolizina, su procedimiento de preparacion y su aplicacion en terapeutica - Google Patents

Derivados de indolizina, su procedimiento de preparacion y su aplicacion en terapeutica

Info

Publication number
PE20130386A1
PE20130386A1 PE2013000019A PE2013000019A PE20130386A1 PE 20130386 A1 PE20130386 A1 PE 20130386A1 PE 2013000019 A PE2013000019 A PE 2013000019A PE 2013000019 A PE2013000019 A PE 2013000019A PE 20130386 A1 PE20130386 A1 PE 20130386A1
Authority
PE
Peru
Prior art keywords
alkyl
methylindolizin
rent
carbonyl
phenyl
Prior art date
Application number
PE2013000019A
Other languages
English (en)
Inventor
Chantal Alcouffe
Corentin Herbert
Gilbert Lassalle
Original Assignee
Sanofi Sa
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=43382527&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20130386(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Sanofi Sa filed Critical Sanofi Sa
Publication of PE20130386A1 publication Critical patent/PE20130386A1/es

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    • C07ORGANIC CHEMISTRY
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    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-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
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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
    • A61K31/437Heterocyclic 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 containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/4709Non-condensed quinolines and containing further heterocyclic rings
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    • 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
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
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    • 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
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    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • A61K9/2018Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
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    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
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    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2059Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/30Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/32Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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    • C07DHETEROCYCLIC COMPOUNDS
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    • C07D207/30Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/34Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members 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
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    • C07D211/80Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D211/82Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms

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Abstract

SE REFIERE A COMPUESTOS DERIVADOS DE INDOLIZINA DE FORMULA (I) DONDE R1 ES H, HALOGENO, ALQUILO SUSTITUIDO OPCIONALMENTE CON -COOR5, ALQUENILO SUSTITUIDO OPCIONALMENTE CON -COOR5, ENTRE OTROS, EN DONDE R5 ES H, HALOGENOALQUILO, CICLOALQUILO, ENTRE OTROS; R2 ES H, ALQUILO O FENILO SUSTITUIDO OPCIONALMENTE CON ALQUILO; R3 Y R4 FORMAN JUNTO CON LOS ATOMOS DE CARBONO DEL NUCLEO FENILO AL QUE ESTAN UNIDOS UN HETEROCICLO NITROGENADO DE 6 MIEMBROS DE FORMULA (A), (B), ENTRE OTROS, DONDE Ra ES H, ALQUILO, HALOGENOALQUILO, ENTRE OTROS; Ra' ES H, ALQUILO, ENTRE OTROS; Rb ES H, ALQUILO, ENTRE OTROS; Rb' ES H, ALQUILO, CICLOALQUILO, FENILO, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: 2-{6-[(1-METOXI-2-METILINDOLIZIN-3-IL)CARBONIL]-2,4-DIOXO-1,4-DIHIDROQUINAZOLIN-3(2H)-IL}-N,N'-DIMETILACETAMIDA; 6-[(1-METOXI-2-METILINDOLIZIN-3-IL)CARBONIL]-3-[(3-METIL-1,2,4-OXADIAZOL-5-IL)METIL]QUINAZOLINA-2,4(1H,3H)-DIONA; ACIDO 3-{3-(2,4-DIOXO-3-PROPIL-1,2,3,4-TETRAHIDROQUINAZOLIN-6-IL)CARBONIL}-2-METILINDOLIZIN-1-IL}BENZOICO; ENTRE OTROS. TAMBIEN SE REFIERE A UN PROCEDIMIENTO DE PREPARACION Y A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE LOS FACTORES DE CRECIMIENTO DE FIBROBLASTOS (FGF) SIENDO UTILES EN EL TRATAMIENTO DE ATEROSCLEROSIS, FIBROSIS HEPATICA, CANCER
PE2013000019A 2010-07-06 2011-07-04 Derivados de indolizina, su procedimiento de preparacion y su aplicacion en terapeutica PE20130386A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
FR1055477A FR2962438B1 (fr) 2010-07-06 2010-07-06 Derives d'indolizines, procedes de preparation et application en therapeutique

Publications (1)

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PE20130386A1 true PE20130386A1 (es) 2013-04-11

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PE2013000019A PE20130386A1 (es) 2010-07-06 2011-07-04 Derivados de indolizina, su procedimiento de preparacion y su aplicacion en terapeutica

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US (1) US8859544B2 (es)
EP (1) EP2590975B1 (es)
JP (1) JP5863788B2 (es)
KR (1) KR101797795B1 (es)
CN (1) CN103080112B (es)
AR (1) AR082768A1 (es)
AU (1) AU2011275426B2 (es)
BR (1) BR112013000306A2 (es)
CA (1) CA2805065C (es)
CL (1) CL2013000018A1 (es)
CO (1) CO6650361A2 (es)
CR (1) CR20130001A (es)
CY (1) CY1116945T1 (es)
DK (1) DK2590975T3 (es)
DO (1) DOP2012000321A (es)
EA (1) EA024160B1 (es)
EC (1) ECSP13012362A (es)
ES (1) ES2552850T3 (es)
FR (1) FR2962438B1 (es)
GT (1) GT201300001A (es)
HR (1) HRP20151162T1 (es)
HU (1) HUE026067T2 (es)
IL (1) IL223844A (es)
MA (1) MA34451B1 (es)
MX (1) MX2012015306A (es)
MY (1) MY163202A (es)
NI (1) NI201200191A (es)
PE (1) PE20130386A1 (es)
PH (1) PH12013500005A1 (es)
PL (1) PL2590975T3 (es)
PT (1) PT2590975E (es)
SG (2) SG10201505282YA (es)
SI (1) SI2590975T1 (es)
TN (1) TN2012000609A1 (es)
TW (1) TWI494310B (es)
UA (1) UA109013C2 (es)
UY (1) UY33489A (es)
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WO2012088266A2 (en) 2010-12-22 2012-06-28 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3
FR2985258A1 (fr) * 2011-12-28 2013-07-05 Sanofi Sa Composes dimeres agonistes des recepteurs des fgfs (fgfrs), leur procede de preparation et leur application en therapeutique
UA125503C2 (uk) 2012-06-13 2022-04-13 Інсайт Холдинґс Корпорейшн Заміщені трициклічні сполуки як інгібітори fgfr
WO2014026125A1 (en) 2012-08-10 2014-02-13 Incyte Corporation Pyrazine derivatives as fgfr inhibitors
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
WO2014172644A2 (en) 2013-04-19 2014-10-23 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
US10435402B2 (en) * 2015-01-08 2019-10-08 Advinus Therapeutics Limited Bicyclic compounds, compositions and medicinal applications thereof
UA121669C2 (uk) 2015-02-20 2020-07-10 Інсайт Корпорейшн Біциклічні гетероцикли як інгібітори fgfr
US9580423B2 (en) 2015-02-20 2017-02-28 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
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