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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
Authority
AR
Argentina
Prior art keywords
alk
group
coor5
alkyl
groups
Prior art date
Application number
ARP110102399A
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English (en)
Inventor
Chantal Alcouffe
Corentin Herbert
Gilbert Lassale
Original Assignee
Sanofi Sa
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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=AR082768(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 AR082768A1 publication Critical patent/AR082768A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • 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
    • 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/4709Non-condensed quinolines and containing further heterocyclic rings
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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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
    • 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
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
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    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
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    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
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    • A61P17/06Antipsoriatics
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    • A61P19/00Drugs for skeletal disorders
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    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P7/04Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • 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
    • C07D207/34Heterocyclic 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
    • C07D207/36Oxygen or sulfur atoms
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • 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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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Urology & Nephrology (AREA)
  • Obesity (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Oncology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Endocrinology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Vascular Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Neurosurgery (AREA)
  • Pulmonology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Reproductive Health (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)

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)

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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

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AR082768A1 true AR082768A1 (es) 2013-01-09

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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)
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