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AR045887A1 - Antagonistas del receptor cgrp - Google Patents

Antagonistas del receptor cgrp

Info

Publication number
AR045887A1
AR045887A1 ARP040101238A ARP040101238A AR045887A1 AR 045887 A1 AR045887 A1 AR 045887A1 AR P040101238 A ARP040101238 A AR P040101238A AR P040101238 A ARP040101238 A AR P040101238A AR 045887 A1 AR045887 A1 AR 045887A1
Authority
AR
Argentina
Prior art keywords
alkyl
heteroaryl
substituted
unsubstituted
independently selected
Prior art date
Application number
ARP040101238A
Other languages
English (en)
Original Assignee
Merck & Co Inc
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
Application filed by Merck & Co Inc filed Critical Merck & Co Inc
Publication of AR045887A1 publication Critical patent/AR045887A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • 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
    • A61P1/02Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/10Drugs for disorders of the urinary system of the bladder
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/06Antimigraine agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/16Otologicals
    • 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
    • A61P3/08Drugs 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
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/08Plasma substitutes; Perfusion solutions; Dialytics or haemodialytics; Drugs for electrolytic or acid-base disorders, e.g. hypovolemic shock
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Pulmonology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Psychiatry (AREA)
  • Cardiology (AREA)
  • Communicable Diseases (AREA)
  • Obesity (AREA)
  • Ophthalmology & Optometry (AREA)
  • Addiction (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Oncology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

La presente se refiere a antagonistas del receptor CGRP. Compuestos útiles como antagonistas de los receptores CGRP y útiles en el tratamiento o prevención de enfermedades en las cuales el CGRP está relacionado, tales como dolor de cabeza, migrana y cefaleas en racimos. La presente está también dirigida a composiciones farmacéuticas que comprenden estos compuestos y el uso de estos compuestos y composiciones en la prevención de tales enfermedades en las cuales el CGRP está relacionado. Reivindicación 1: Un compuesto de fórmula (1) donde: R1 se selecciona de: H, alquil C1-6, cicloalquil C3-6 y heterociclo, no sustituido o sustituido con uno o más sustituyentes independientemente seleccionados de: alquil C1-6, cicloalquil C3-6, fenil, heteroaril, heterociclo, (F)p alquil C1-3, halógeno, OR4, O(CH2)sOR4, CO2R4, CN, NR10R11, O(CO)R4, donde dicho fenil, dicho heteroaril y dicho heterociclo están cada uno independientemente no sustituido o sustituido con de 1 a 5 sustituyentes donde los sustituyentes son independientemente seleccionados entre R4, donde dicho heteroaril se selecciona entre imidazol, isoxazol, oxazol, pirazina, pirazol, piridazina, piridina, pirimidina, y tiazol, donde dicho heterociclo se selecciona entre azetidina, dioxano, dioxolano, morfolina, oxetano, piperazina, piperidina, pirrolidina, tetrahidrofurano y tetrahidropirano; aril, o heteroaril seleccionado entre: fenil, imidazol, isoxazol, oxazol, pirazina, pirazol, piridazina, piridina, pirimidina, y tiazol; donde dicho aril y dicho heteroaril están cada uno independientemente no sustituido o sustituido con uno o más sustituyentes independientemente seleccionados entre alquil C1-6, cicloalquil C3-6, (F)p alquil C1-3, halógeno, OR4, CO2R4, (CO)NR10R11, SO2NR10R11, N(R10)SO2R11, S(O)mR4, CN, NR10R11 y O(CO)R4; R2 se selecciona entre: H alquil C0-6, cicloalquil C3-6 y heterociclo, no sustituido o sustituido con uno o más sustituyentes independientemente seleccionados entre: alquil C1-6, cicloalquil C3-6, fenil, heteroaril, heterociclo, (F)p alquil C1-3, halógeno, OR4, O(CH2)sOR4, CO2R4, CN, NR10R11 y O(CO)R4, donde dicho fenil, dicho heteroaril, y dicho heterociclo cada uno independientemente se encuentra no sustituido o sustituido con de 1 a 5 sustituyentes independientemente seleccionados de R4; donde dicho heteroaril se selecciona entre: benzimidazol, benzotiofeno, furano, imidazol, indol, isoxazol, oxazol, pirazina, pirazol, piridazina, piridina, pirimidina, pirrol, tiazol, tiofeno, y triazol; donde dicho heterociclo se selecciona entre: azetidina, imidazolidina, imidazolina, isoxazolina, isoxazolidina, morfolina, oxazolina, oxazolidina, oxetano, pirazolidina, pirazolina, pirrolina, tetrahidrofurano, tetrahidripirano, tiazolina, y tiazolidina, aril o heteroaril, seleccionados entre fenil, benzimidazol, benzotiofeno, furano, imidazol, indol, isoxazol, oxazol, pirazina, pirazol, piridazina, piridina, pirimidina, pirrol, tiazol, tiofeno, y triazol; donde dicho arilo y dicho heteroarilo están cada uno independientemente no sustituidos o sustituidos con uno o más sustituyentes independientemente seleccionados entre alquil C1-6, cicloalquil C3-6, (F)p alquil C1- 3, halógeno, OR4, CO2R4, (CO)NR10R11, SO2NR10R11, N(R10)SO2R11, S(O)mR4, CN, NR10R11 y O(CO)R4; R10 y R11 están independientemente seleccionados entre H, alquil C1-6, (F)p alquil C1-6, cicloalquil C3-6, aril, heteroaril y benzil, no sustituido o sustituido con halógeno, hidróxido o alcoxi C1-6 donde R10 y R11 pueden estar unidos para formar un anillo seleccionado entre azetidinil, pirrolidinil, piperidinil, piperazinil y morfolinil, el cual no está sustituido o está sustituido con de 1 a 5 sustituyentes que están independientemente seleccionados entre R4; R4 está independientemente seleccionado entre H, alquil C1-6, (F)p alquil C1-6, cicloalquil C3-6, aril, heteroaril y fenil, no sustituido o sustituido con hidroxi o alcoxi C1-6; R3 está independientemente seleccionado entre H, alquil C1-3 no sustituido o sustituido, CN y CO2R4; p es 0a 2q+1, para un sustituyente con q carbonos; m es 0, 1 o 2; s es 1, 2 o 3. Y sales farmacéuticamente aceptables y diastereómeros individuales de ellos.
ARP040101238A 2003-04-15 2004-04-13 Antagonistas del receptor cgrp AR045887A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US46308903P 2003-04-15 2003-04-15
US51035203P 2003-10-10 2003-10-10

Publications (1)

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AR045887A1 true AR045887A1 (es) 2005-11-16

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US (6) US6953790B2 (es)
EP (2) EP1638969B1 (es)
JP (1) JP3967766B2 (es)
KR (1) KR100769030B1 (es)
CN (1) CN100384843C (es)
AR (1) AR045887A1 (es)
AT (1) ATE413400T1 (es)
AU (1) AU2004230926B2 (es)
BR (1) BRPI0409601A (es)
CA (1) CA2522220C (es)
CL (1) CL2004000788A1 (es)
CO (1) CO5640130A2 (es)
CY (1) CY1108714T1 (es)
DE (1) DE602004017608D1 (es)
DK (1) DK1638969T3 (es)
EC (1) ECSP056097A (es)
ES (1) ES2314417T3 (es)
HR (1) HRP20080666T3 (es)
IS (1) IS2759B (es)
JO (1) JO2355B1 (es)
MA (1) MA27728A1 (es)
MX (1) MXPA05011166A (es)
NO (1) NO327655B1 (es)
NZ (1) NZ543357A (es)
PE (1) PE20050020A1 (es)
PL (1) PL1638969T3 (es)
PT (1) PT1638969E (es)
RU (1) RU2308458C2 (es)
SI (1) SI1638969T1 (es)
TW (1) TWI314931B (es)
UA (1) UA82877C2 (es)
WO (2) WO2004092168A1 (es)

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