AR082768A1 - Derivados de indolizina, su procedimiento de preparacion y composiciones farmaceuticas que los contienen - Google Patents

Derivados de indolizina, su procedimiento de preparacion y composiciones farmaceuticas que los contienen

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Publication number
AR082768A1
AR082768A1 ARP110102399A ARP110102399A AR082768A1 AR 082768 A1 AR082768 A1 AR 082768A1 AR P110102399 A ARP110102399 A AR P110102399A AR P110102399 A ARP110102399 A AR P110102399A AR 082768 A1 AR082768 A1 AR 082768A1
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AR
Argentina
Prior art keywords
alk
group
coor5
alkyl
groups
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ARP110102399A
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English (en)
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Chantal Alcouffe
Corentin Herbert
Gilbert Lassale
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Sanofi Sa
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Application filed by Sanofi Sa filed Critical Sanofi Sa
Publication of AR082768A1 publication Critical patent/AR082768A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—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
    • A61K31/437—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 containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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    • 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
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
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    • A61K31/33—Heterocyclic compounds
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    • 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
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    • 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
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    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
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    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
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    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
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    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
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    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
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    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic 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
    • C07D207/30—Heterocyclic 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
    • C07D207/32—Heterocyclic 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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    • C07D207/30—Heterocyclic 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
    • C07D207/34—Heterocyclic 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
    • C07D207/36—Oxygen or sulfur atoms
    • C—CHEMISTRY; METALLURGY
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    • C07D211/80—Heterocyclic 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
    • C07D211/82—Heterocyclic 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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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
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  • Animal Behavior & Ethology (AREA)
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  • Diabetes (AREA)
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  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Obesity (AREA)
  • Pain & Pain Management (AREA)
  • Oncology (AREA)
  • Endocrinology (AREA)
  • Dermatology (AREA)
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  • Immunology (AREA)
  • Neurology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Neurosurgery (AREA)
  • Vascular Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
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Abstract

Reivindicación 1: Compuesto de fórmula (1) en la que R1 representa un átomo de hidrógeno o de halógeno, un grupo alquilo sustituido opcionalmente con -COOR5, alquenilo sustituido opcionalmente con -COOR5, un grupo -COOR5, -CONR5R6, -NR5COR6, -NR5-SO2R6, -OR5, -O-Alk-OR5, -O-Alk-COOR5, -O-Alk-OR5, -O-Alk-NR5R6, -O-Alk-NR7R8, o un grupo arilo, en particular fenilo, o heteroarilo, estando dicho grupo arilo o heteroarilo sustituido opcionalmente con uno o varios grupos elegidos entre los átomos de halógeno, los grupos alquilo, los grupos cicloalquilo, -COOR5, -CF3, -OCF3, -CN, -C(NH2)NOH, -OR5, -O-Alk-COOR5, -O-Alk-NR5R6, -O-Alk-NR7R8, -Alk-OR5, -Alk-COOR5, -CONR5R6, -CO-NR5-OR6, -CO-NR5-SO2R7, -CONR5-Alk-NR5R6, -CONR5-Alk-NR7R8, -Alk-NR5R6, -NR5R6, -NC(O)N(CH3)2, -CO-Alk, -CO(OAlk)nOH, -COO-AIkNR5R6, COOAlk-NR7R8 y los grupos heteroarilo de 5 eslabones, estando dichos grupos heteroarilo sustituidos opcionalmente con uno o varios grupos elegidos entre los átomos de halógeno y los grupos alquilo, -CF3, -CN, -COOR5, -Alk-OR5, -Alk-COOR5, -CONR5R6, -CONR7R8, -CO-NR5-OR6, -CO-NR5-SO2R7 y -NR5R5, -Alk-NR5R6, o con un grupo hidroxilo o con un átomo de oxígeno; n es un número entero que va de 1 a 3; R2 representa un átomo de hidrógeno, un grupo alquilo, un grupo fenilo sustituido opcionalmente con uno o varios grupos alquilo, R3 y R4 forman conjuntamente, con los átomos de carbono del núcleo fenilo al que están unidos, un heterociclo nitrogenado de 6 eslabones que responde a una de las fórmulas (A), (B) ó (C) en las que los trazos ondulados representan el núcleo fenilo al que están unidos R3 y R4; y Ra representa un átomo de hidrógeno o un grupo alquilo, halógenoalquilo, -Alk-CF3, -Alk-COOR5, -Alk’-COOR5, -Alk-CONR5R6, -Alk’-CONR5R6, -Alk-CONR7R8, -Alk-NR5R6, -AIkCONR5-OR6, -Alk-NR7R8, -Alk-cicloalquilo, -Alk-OR5, -Alk-S-R5, -Alk-CN, -OR5, -OAIkCOOR5, -NR5R6, -NR5-COOR6, -Alk-arilo, -Alk-O-arilo, -Alk-O-heteroarilo, -Alk-heteroarilo o heteroarilo en el que el grupo arilo o heteroarilo está sustituido opcionalmente con uno o varios átomos de halógeno y/o grupos alquilo, cicloalquilo, -CF3, -OCF3, -O-R5 o -S-R5; Ra’ representa un átomo de hidrógeno o un grupo alquilo, lineal, ramificado, cíclico o parcialmente cíclico, o un grupo -Alk-OR5 o -Alk-NR5R6, -Alk-NR7R8, estando Ra’ sustituido opcionalmente con uno o varios átomos de halógeno; Rb representa un átomo de hidrógeno o un grupo alquilo o -Alk-COOR5; Rb’ representa un átomo de hidrógeno o un grupo alquilo, halógenoalquilo, cicloalquilo, fenilo o -Alk-COOR5; Rc representa un átomo de hidrógeno o un grupo alquilo, -CN, -COOR5, -CO-NR5R5, -CONR7R8, -CO-NR5-Alk-NR5R6, -CONR5-Alk-OR5, CONR5SO2R5, o -Alk-arilo, -Alk-heteroarilo, en el que el grupo arilo o heteroarilo está sustituido opcionalmente con uno o varios átomos de halógeno y/o grupos alquilo, cicloalquilo, -CF3, -OCF3, -O-alquilo o -S-alquilo; Rc’ representa un átomo de hidrógeno o un grupo alquilo; Rc’’ representa un átomo de hidrógeno o un grupo alquilo, alquenilo, halógenoalquilo, cicloalquilo, -Alk-NR5R6, -Alk-NR7R8, -Alk-OR5, -Alk-SR5; R5 y R6, idénticos o diferentes, representan átomos de hidrógeno, grupos halógenoalquilo o grupos alquilo, grupos cicloalquilo, un grupo Ms; R7 y R8, idénticos o diferentes, representan átomos de hidrógeno o grupos alquilo o fenilo, o bien R7 y R8 forman conjuntamente un ciclo saturado de 3 a 8 eslabones que puede contener opcionalmente un heteroátomo; Alk representa una cadena alquileno lineal o ramificada; y Alk’ representa una cadena alquileno lineal, ramificada, cíclica o parcialmente cíclica; opcionalmente en la forma de una de sus sales farmacéuticamente aceptables.
ARP110102399A 2010-07-06 2011-07-05 Derivados de indolizina, su procedimiento de preparacion y composiciones farmaceuticas que los contienen AR082768A1 (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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AR082768A1 true AR082768A1 (es) 2013-01-09

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MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
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CN106045994A (zh) * 2016-06-12 2016-10-26 上海大学 全氟烷基吲嗪衍生物及其合成方法
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DOP2012000321A (es) 2013-04-15
CA2805065C (en) 2018-07-03
EA024160B1 (ru) 2016-08-31
NI201200191A (es) 2013-05-13
TWI494310B (zh) 2015-08-01
ES2552850T3 (es) 2015-12-02
UA109013C2 (en) 2015-07-10
SG10201505282YA (en) 2015-08-28
PT2590975E (pt) 2015-11-24
CY1116945T1 (el) 2017-04-05
DK2590975T3 (en) 2015-12-07
BR112013000306A2 (pt) 2020-08-04
PL2590975T3 (pl) 2016-01-29
CL2013000018A1 (es) 2013-05-10
MA34451B1 (fr) 2013-08-01
TN2012000609A1 (en) 2014-04-01
WO2012004731A1 (en) 2012-01-12
AU2011275426A1 (en) 2013-01-24
CO6650361A2 (es) 2013-04-15
GT201300001A (es) 2014-04-29
AU2011275426B2 (en) 2016-05-12
UY33489A (es) 2012-01-31
EA201291409A1 (ru) 2013-05-30
MX2012015306A (es) 2013-04-29
KR20130128362A (ko) 2013-11-26
MY163202A (en) 2017-08-15
CA2805065A1 (en) 2012-01-12
JP5863788B2 (ja) 2016-02-17
FR2962438A1 (fr) 2012-01-13
ECSP13012362A (es) 2013-01-31
HRP20151162T1 (hr) 2015-12-04
EP2590975B1 (en) 2015-08-19
CN103080112A (zh) 2013-05-01
TW201206931A (en) 2012-02-16
CN103080112B (zh) 2016-04-20
JP2013530210A (ja) 2013-07-25
US20130116249A1 (en) 2013-05-09
IL223844A (en) 2016-03-31
HUE026067T2 (en) 2016-05-30
SG186436A1 (en) 2013-01-30
SI2590975T1 (sl) 2015-12-31
CR20130001A (es) 2013-02-05
KR101797795B1 (ko) 2017-11-15
FR2962438B1 (fr) 2012-08-17
EP2590975A1 (en) 2013-05-15
PE20130386A1 (es) 2013-04-11
US8859544B2 (en) 2014-10-14
ZA201300100B (en) 2014-03-26

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