AR074109A1 - Pirrolidinas heterociclicas agonistas de receptores de la melanocortina, composiciones farmaceuticas que las contienen y uso de las mismas en el tratamiento de la obesidad, diabetes y disfuncion erectil. - Google Patents

Pirrolidinas heterociclicas agonistas de receptores de la melanocortina, composiciones farmaceuticas que las contienen y uso de las mismas en el tratamiento de la obesidad, diabetes y disfuncion erectil.

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Publication number
AR074109A1
AR074109A1 ARP090104355A ARP090104355A AR074109A1 AR 074109 A1 AR074109 A1 AR 074109A1 AR P090104355 A ARP090104355 A AR P090104355A AR P090104355 A ARP090104355 A AR P090104355A AR 074109 A1 AR074109 A1 AR 074109A1
Authority
AR
Argentina
Prior art keywords
alkyl
unsubstituted
hydroxy
group
trifluoromethyl
Prior art date
Application number
ARP090104355A
Other languages
English (en)
Inventor
Dong Sup Shim
Koo Lee
Sung-Pil Choi
Sang Dae Lee
Sang Pil Moon
In Ae Ahn
Soo Yong Chung
Hyun Min Lee
Original Assignee
Lg Life Sciences Ltd
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Filing date
Publication date
Application filed by Lg Life Sciences Ltd filed Critical Lg Life Sciences Ltd
Publication of AR074109A1 publication Critical patent/AR074109A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero 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
    • A61K31/40Heterocyclic 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
    • A61K31/4025Heterocyclic 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 not condensed and containing further heterocyclic rings, e.g. cromakalim
    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10Drugs for genital or sexual disorders; Contraceptives for impotence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • A61P27/06Antiglaucoma agents or miotics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • 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
    • 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
    • C07D207/04Heterocyclic 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 no double bonds between ring members or between ring members and non-ring members
    • C07D207/10Heterocyclic 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 no 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
    • C07D207/16Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Reproductive Health (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Emergency Medicine (AREA)
  • Gynecology & Obstetrics (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Hydrogenated Pyridines (AREA)
  • Pyrrole Compounds (AREA)

Abstract

Reivindicacion 1: Un compuesto de la formula (1) caracterizado porque: R1 representa H, o representa alquilo C1-10, cicloalquilo C3-7, arilo C6-10, un heterociclo o un heteroarilo, cada uno de los cuales es insustituido o sustituido con por lo menos un sustituyente seleccionado entre el grupo que consiste en halogeno, amino, alquilo C1-4, trifluorometilo, hidroxi, alcoxi C1-4, ciano y oxo; R2 representa fenilo o un heteroarilo de 6 miembros, cada uno de los cuales es insustituido o mono- o disustituido con uno o más sustituyentes seleccionados entre el grupo que consiste en halogeno, hidroxi, alquilo C1-4, alcoxi C1-4, ciano y amino; R3 representa H, o representa alquilo C1-6 o cicloalquilo C3-7, cada uno de los cuales es insustituido o sustituido con uno o más sustituyentes seleccionados entre el grupo que consiste en halogeno, metilo, trifluorometilo, hidroxi y amino; R4 representa cicloalquilo C4-7 o un heterociclo monocíclico, cada uno de los cuales es insustituido o mono- o poli-sustituido con uno o más sustituyentes seleccionados entre el grupo que consiste en halogeno, hidroxi, alquilo C1-4, trifluorometilo, alcoxi C1-4 y oxo; o representa fenilo o un heteroarilo de seis miembros, cada uno de los cuales es insustituido o mono- o di-sustituido con uno o más sustituyentes seleccionados entre el grupo que consiste en halogeno, hidroxi, alquilo C1-4, trifluorometilo, alcoxi C1-4 y amino; y R5 representa alquilo C1-6, difluorometilo, trifluorometilo, cicloalquilo C3-6, amino, alquilamino C1-4, di-alquilo C1-4amino, fenilo, un heteroarilo monocíclico o un heterociclo monocíclico en donde el alquilo es insustituido o sustituido con por lo menos un sustituyente seleccionado entre el grupo que consiste en fluoro, hidroxi, mercapto, alcoxi C1-4, acetoxi, amino, acetilamino, ciano, carbamoilo, dimetil carbamoilo y oxo y fenilo o el heteroarilo es insustituido o mono- o di- sustituido con uno o más sustituyentes seleccionados entre el grupo que consiste en halogeno, hidroxi, metilo, trifluorometilo, metoxi y amino, o una sal farmacéuticamente aceptable o un isomero del mismo.
ARP090104355A 2008-11-12 2009-11-11 Pirrolidinas heterociclicas agonistas de receptores de la melanocortina, composiciones farmaceuticas que las contienen y uso de las mismas en el tratamiento de la obesidad, diabetes y disfuncion erectil. AR074109A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
KR20080112403 2008-11-12

Publications (1)

Publication Number Publication Date
AR074109A1 true AR074109A1 (es) 2010-12-22

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ARP090104355A AR074109A1 (es) 2008-11-12 2009-11-11 Pirrolidinas heterociclicas agonistas de receptores de la melanocortina, composiciones farmaceuticas que las contienen y uso de las mismas en el tratamiento de la obesidad, diabetes y disfuncion erectil.

Country Status (26)

Country Link
US (4) US8288386B2 (es)
EP (1) EP2350060B1 (es)
JP (1) JP5399506B2 (es)
KR (1) KR101141976B1 (es)
CN (1) CN102282141B (es)
AR (1) AR074109A1 (es)
AU (1) AU2009314827B2 (es)
BR (1) BRPI0921063B8 (es)
CA (1) CA2742248C (es)
CL (1) CL2011001073A1 (es)
CO (1) CO6362006A2 (es)
CR (1) CR20110250A (es)
EA (1) EA019146B1 (es)
EC (1) ECSP11011026A (es)
GE (1) GEP20135850B (es)
IL (1) IL212468A0 (es)
MA (1) MA32774B1 (es)
MX (1) MX2011004583A (es)
NZ (1) NZ592512A (es)
PE (1) PE20110684A1 (es)
TN (1) TN2011000222A1 (es)
TW (1) TWI389903B (es)
UA (1) UA99555C2 (es)
UY (1) UY32238A (es)
WO (1) WO2010056022A2 (es)
ZA (1) ZA201103154B (es)

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