AR073631A1 - Antagonistas del receptor transitorio potencial de vanilloides 1 ( trpv1) utiles para tratar inflamacion y dolor - Google Patents

Antagonistas del receptor transitorio potencial de vanilloides 1 ( trpv1) utiles para tratar inflamacion y dolor

Info

Publication number
AR073631A1
AR073631A1 ARP090103975A ARP090103975A AR073631A1 AR 073631 A1 AR073631 A1 AR 073631A1 AR P090103975 A ARP090103975 A AR P090103975A AR P090103975 A ARP090103975 A AR P090103975A AR 073631 A1 AR073631 A1 AR 073631A1
Authority
AR
Argentina
Prior art keywords
dihydro
urea
indazol
chromen
benzopyran
Prior art date
Application number
ARP090103975A
Other languages
English (en)
Inventor
Robert G Schimidt
Arthur R Gomtsyan
Eric A Voight
Michael E Kort
Philip R Kym
Heath A Mcdonald
Erol K Bayburt
Jun Chen
Jerome F Daanen
Jr Stanley Didomenico
Richard J Perner
Original Assignee
Abbott Lab
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 Abbott Lab filed Critical Abbott Lab
Publication of AR073631A1 publication Critical patent/AR073631A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D311/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
    • C07D311/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D311/74—Benzo[b]pyrans, hydrogenated in the carbocyclic ring
    • 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
    • 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
    • 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
    • A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • 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
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/08—Bronchodilators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/14—Antitussive agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/10—Drugs for disorders of the urinary system of the bladder
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • 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
    • C07D405/00—Heterocyclic 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
    • C07D405/02—Heterocyclic 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 two hetero rings
    • C07D405/12—Heterocyclic 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 two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • Urology & Nephrology (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Vascular Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Child & Adolescent Psychology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Pain & Pain Management (AREA)
  • Dermatology (AREA)
  • Immunology (AREA)
  • Biomedical Technology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Otolaryngology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pyrane Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Reivindicacion 1: Un compuesto caracterizado porque responde a la formula (1) o una sal solvato, prodroga, sal de una prodroga aceptables para uso farmacéutico, o una combinacion de los mismos, donde R1 representa un grupo de formula (a), (b), (c) o (d); Rx, en cada caso, representa sustituyente(s) opcional(es) sobre cualquier posicion sustituible del anillo bicíclico seleccionados entre el grupo que consiste de alquilo, halogeno, haloalquilo, OH, O(alquilo), O(haloalquilo), NH2, N(H)(alquilo), y N(alquilo)2; Ra es hidrogeno o metilo; R2 y R3 son iguales o diferentes, y son cada uno en forma independiente hidrogeno, alquilo C1-5, o haloalquilo; o R2 y R3, junto con el átomo de carbono al cual se encuentran unidos, forman un anillo cicloalquilo monocíclico de 3 a 6 átomos de carbono, opcionalmente sustituido con 1, 2 o 3 sustituyentes seleccionados entre el grupo que consiste de alquilo y halogeno; R4 en cada caso, representa sustituyente(s) opcional(es) sobre cualquier posicion sustituible del anillo bicíclico seleccionados entre el grupo que consiste de alquilo, halogeno, haloalquilo, O(alquilo), O(haloalquilo), y SCF3; y m y n son cada uno en forma independiente 0, 1, 2 o 3; con la condicion de que el compuesto no es N-(7-tert-butil-3,4-dihidro-2H-cromen-4-il)-N'-1H-indazol-4-ilurea; N-1H-indazol-4-il-N'-[7-(trifluorometil)-3,4-dihidro-2H-cromen-4-il]urea; N-isoquinolin-5-il-N'-[7-(trifluorometil)-3,4-dihidro-2H-cromen-4-il]urea; N-1H-indazol-4-il-N'-(6-metil-3,4-dihidro-2H-cromen-4-il)urea; N-isoquinolin-5-il-N'-(6-metil-3,4-dihidro-2H-cromen-4-il)urea; N-(6-fluoro-3,4-dihidro-2H-cromen-4-il)-N'-1H-indazol-4-ilurea; N-(6-fluoro-3,4-dihidro-2H-cromen-4-il)-N'-isoquinolin-5-ilurea; N-(6-cloro-7-metil-3,4-dihidro-2H-cromen-4-il)-N'-1H-indazol-4-ilurea; N-(6-cloro-7-metil-3,4-dihidro-2H-cromen-4-il)-N'-isoquinolin-5-ilurea; N-3,4-dihidro-2H-cromen-4-il-N'-1H-indazol-4-ilurea; N-(7-tert-butil-3,4-dihidro-2H-cromen-4-il)-N'-(3metilisoquinolin-5-il)urea; N-(6-fluoro-3,4-dihidro-2H-cromen-4-il)-N'-(3-metilisoquinolin-5-il)urea; N-(6-metil-3,4-dihidro-2H-cromen-4-il)-N'-(3-metilisoquinolin-5-il)urea; N-isoquinolin-5-il-N'-(8-piperidin-1-il-3,4-dihidro-2H-cromen-4-il)urea; N-3,4-dihidro-2H-cromen-4-il-N'-isoquinolin-5-ilurea; (+)-N-isoquinolin-5-il-N'-[7-(trifluorometil)-3,4-dihidro-2H-cromen-4-il]urea; (-)-N-isoquinolin-5-il-N'-[7-(trifluorometil)-3,4-dihidro-2H-cromen-4-il]urea; N-1H-indazol-4-il-N'-[8-(trifluorometil)-3,4-dihidro-2H-cromen-4-il]urea; (-)-N-1H-indazol-4-il-N'-[7-(trifluorometil)-3,4-dihidro-2H-cromen-4-il]urea; (+)-N-1H-indazol-4-il-N'-[7-(trifluorometil)-3,4-dihidro-2H-cromen-4-il]urea; N-1H-indazol-4-il-N'-(8-piperidin-1-il-3,4-dihidro-2H-cromen-4-il)urea; N-(8-tert-butil-3,4-dihidro-2H-cromen-4-il)-N'-1H-indazol-4-ilurea; N-[8-cloro-7-(trifluorometil)-3,4-dihidro-2H-cromen-4-il]-N'-1H-indazol-4-ilurea; (+)-N-(8-tert-butil-3,4-dihidro-2H-cromen-4-il)-N'-1H-indazol-4-ilurea; (-)-N-(8-tert-butil-3,4-dihidro-2H-cromen-4-il)-N'-1H-indazol-4-ilurea; N-1H-indazol-4-il-N'-[8-(trifluorometoxi)-3,4-dihidro-2H-cromen-4-il]urea; N-[8-fluoro-7-(trifluorometil)-3,4-dihidro-2H-cromen-4-il]-N'-1H-indazol-4-ilurea; N-1H-indazol-4-il-N'-[7-(trifluorometoxi)-3,4-dihidro-2H-cromen-4-il]urea; N-(6-fluoro-2-metil-3,4-dihidro-2H-cromen-4-il)-N'-1H-indazol-4-ilurea; N-1H-indazol-4-il-N'-(7-metoxi-2,2-dimetil-3,4-dihidro-2H-cromen-4-il)urea; N-1H-indazol-4-il-N'-(7-metoxi-2,2,8-trimetil-3,4-dihidro-2H-cromen-4-il)urea; N-1H-indazol-4-il-N'-(2,2,8-trimetil-3,4-dihidro-2H-cromen-4-il)urea; N-1H-indazol-4-il-N'-(7-metoxi-2,2-dimetil-8-propil-3,4-dihidro-2H-cromen-4-il)urea; N-(2,2-dimetil-3,4-dihidro-2H-cromen-4-il)-N'-1H-indazol-4-ilurea; N-(7-fluoro-2,2-dimetil-3,4-dihidro-2H-cromen-4-il)-N'-1H-indazol-4-ilurea; N-(7-fluoro-2,2-dietil-3,4-dihidro-2H-cromen-4-il)-N'-1H-indazol-4-ilurea; N-(7,8-difluoro-2,2-dimetil-3,4-dihidro-2H-cromen-4-il)-N'-1H-indazol-4-ilurea; N-(7-(3,3-dimetilbutil)-3,4-dihidro-2H-cromen-4-il)-N'-1H-indazol-4-ilurea; N-(7-tert-butil-2,2-dimetil-3,4-dihidro-2H-cromen-4-il)-N'-1H-indazol-4-ilurea; N-(2,2-dietil-7-fluoro-3,4-dihidro-2H-cromen-4-il)-N'-(1-metil-1H-indazol-4-il)urea; N-(7,8-difluoro-3,4-dihidro-2H-cromen-4-il)-N'-1H-indazol-4-ilurea; N-(7-fluoro-2,2-dipropil-3,4-dihidro-2H-cromen-4-il)-N'-1H-indazol-4-ilurea; N-(2,2-dibutil-7-fluoro-3,4-dihidro-2H-cromen-4-il)-N'-1H-indazol-4-ilurea; N-(2-tert-butil-7-fluoro-3,4-dihidro-2H-cromen-4-il)-N'-1H-indazol-4-ilurea; N-(2-tert-butil-7-fluoro-3,4-dihidro-2H-cromen-4-il)-N'-(1-metil-1H-indazol-4-il)urea; N-(8-tert-butil-3,4-dihidro-2H-cromen-4-il)-N'-(7-hidroxi-5,6,7,8-tetrahidronaftalen-1-il)urea; N-(7-hidroxi-5,6,7,8-tetrahidronaftalen-1-il)-N'-(6-metil-3,4-dihidro-2H-cromen-4-il)urea; N-[(4R)-3,4-dihidro-2H-cromen-4-il]-N'-(7-hidroxi-5,6,7,8-tetrahidronaftalen-1-il)urea; N-[(4S)-3,4-dihidro-2H-cromen-4-il]-N'-(7-hidroxi-5,6,7,8-tetrahidronaftalen-1-il)urea; 1-(1H-indazol-4-il)-3-(espiro[croman-2,1'-ciclohexan]-4-il)urea; 1-(7-fluoroespiro[croman-2,1'-ciclohexan]-4-il)-3-(1H-indazol-4-il)urea; 1-(7-fluoroespiro[croman-2,1'-cicIobutan]-4-il)-3-(1H-indazol-4-il)urea; 1-(7-fluoroespiro[croman-2,1'-ciclobutan]-4-il)-3-(1-metil-1H-indazol-4-il)urea; 1-(6,7-dimetilespiro[croman-2,1'-ciclohexan]-4-il)-3-(1H-indazol-4-il)urea; 1-(6,8-dicloroespiro[croman-2,1'-ciclohexan]-4-il)-3-(1H-indazol-4-il)urea; 1-(6-cloroespiro[croman-2,1l-ciclohexan]-4-il)-3-(1H-indazol-4-il)urea; 1-(7-tertbutilespiro[croman-2,1'-ciclobutan]-4-il)-3-(1H-indazol-4-il)urea, 1-(6,8-difluoroespiro[croman-2,1'-ciclohexan]-4-il)-3-(1H-indazol-4-il)urea; 1-(6-etoxiespiro[croman-2,1'-ciclohexan]-4-il)-3-(1H-indazol-4-il)urea; 1-(1H-indazol-4-il)-3-(6-metilespiro[croman-2,1'-ciclopentan]-4-il)urea; 1-(7-etoxiespiro[croman-2,1'-ciclopentan]-4-il)-3-(1H-indazol-4-il)urea; 1-(6,7-dimetilespiro[croman-2,1'-ciclopentan]-4-il)-3-(1H-indazol-4-il)urea; 1-(7-fluoroespiro[croman-2,1l-ciclopentan]-4-il)-3-(1H-indazol-4-il)urea; 1-(1-metil-1H-indazol-4-il)-3-(espiro[croman-2,1'-ciclohexan]-4-il)urea; 1-(1H-indazol-4-il)-3-(7-metoxiespiro[croman-2,1'-ciclohexan]-4-il)urea; (+- )1-(3,4-dihidro-2,2-dimetil-2H-1-benzopiran-4-il)-3-(isoquinolin-5-il)urea; (+- )1-(7-cloro-3,4-dihidro-2,2-dimetil-2H-1-benzopiran-4-il)-3-(isoquinolin-5-il)urea; (+- )1-(6-bromo-3,4-dihidro-2,2-dimetil-2H-1-benzopiran-4-il)-3-(isoquinolin-5-il)urea; (+- )1-(6-metoxi-3,4-dihidro-2,2-dimetil-2H-1-benzopiran-4-il)-3-(isoquinolin-5-il)urea; (+- )1-(7-metoxi-3,4-dihidro-2,2-dimetil-2H-1-benzopiran-4-il)-3-(isoquinolin-5-il)urea; (+- )1-(6-metil-3,4-dihidro-2,2-dimetil-2H-1-benzopiran-4-il)-3-(isoquinolin-5-il)urea; (+- )1-(7-metoxi-3,4-dihidro-2,2-dimetil-2H-1-benzopiran-4-il)-3-(1-metilisoquinoIin-5-il)urea; (+- )1-(6-bromo-3,4-dihidro-2,2-dimetil-2H-1-benzopiran-4-il)-3-(1-metilisoquinolin-5-il)urea; (+- )1-(6-metil-3,4-dihidro-2,2-dimetil-2H-1-benzopiran-4-il)-3-(1-metilisoquinolin-5-il)urea; (+- )1-(3,4-dihidro-2,2-dimetil-2H-1-benzopiran-4-il)-3-(1-metilisoquinolin-5-il)urea; (+- )1-(3,4-dihidro-espiro-[2H-1-benzopiran-2,1'-ciclobutan]-4-il)-3-(isoquinolin-5-il)urea; (+)1-(3,4-dihidro-espiro-[2H-1-benzopiran-2,1'-ciclobutan]-4-il)-3-(isoquinolin-5-il)urea; (-)1-(3,4-dihidro-espiro-[2H-1-benzopiran-2,1'-ciclobutan]-4-il)-3-(isoquinolin-5-il)urea; (+- )1-(3,4-dihidro-espiro-[2H-1-benzopiran-2,1'-ciclobutan]-4-il)-3-(8-cloroisoquinolin-5-il)urea; (+- )1-(3,4-dihidro-espiro-[2H-1-benzopiran-2,1'-ciclobutan]-4-il)-3-(3-metilisoquinolin-5-il)urea; (+- )1-(3,4-dihidro-espiro-[2H-1-benzopiran-2,1'-ciclobutan]-4-il)-3-(1-metilisoquinolin-5-il)urea; (+- )1-(3,4-dihidro-6-metil-espiro-[2H-1-benzopiran-2,1'-ciclobutan]-4-il)-3-(isoquinolin-5-il)urea; (+- )1-(3,4-dihidro-7-metil-espiro-[2H-1-benzopiran-2,1'-ciclobutan]-4-il)-3-(isoquinolin-5-il)urea; (+- )1-(3,4-dihidro-6-fluoro-espiro-[2H-1-benzopiran-2,1'-ciclobutan]-4-il)-3-(isoquinolin-5-il)urea; (+)1-(3,4-dihidro-6-fluoro-espiro-[2H-1-benzopiran-2,1'-ciclobutan]-4-il)-3-(isoquinolin-5-il)urea; (-)1-(3,4-dihidro-6-fluoro-espiro-[2H-1-benzopiran-2,1'-ciclobutan]-4-il)-3-(isoquinolin-5-il)urea; (+- )1-(3,4-dihidro-7-metoxi-espiro-[2H-1-benzopiran-2,1'-ciclobutan]-4-il)-3-(isoquinolin-5-il)urea; 1-(6,8-difluoro-3,4-dihidro-espiro-[2H-1-benzopiran-2,1'-ciclobutan]-4-il)-3-(isoquinolin-5-il)urea; (+- )1-(8-cloro-3,4-dihidro-espiro-[2H-1-benzopiran-2,1'-ciclobutan]-4-il)-3-(isoquinolin-5-il)urea; (+- )1-(3,4-dihidro-6-metoxi-espiro-[2H-1-benzopiran-2,1'-ciclobutan]-4-il)-3-(isoquinolin-5-il)urea; clorhidrato de (+- )1-(7-difluorometoxi-3,4-dihidro-espiro-[2H-1-benzopiran-2,1'-ciclobutan]-4-il)-3-(isoquinolin-5-il)urea; (+- )1-(7-difluorometoxi-3,4-dihidro-espiro-[2H-1-benzopiran-2,1'-ciclobutan]-4-il)-3-(3-metilisoquinolin-5-il)urea; (+- )1-(7-cloro-3,4-dihidro-espiro-[2H-1-benzopiran-2,1'-ciclobutan]-4-il)-3-(3-metilisoquinolin-5-il)urea; (+)1-(6,8-difluoro-3,4-dihidro-espiro-[2H-1-benzopiran-2,1'-ciclobutan]-4-il)-3-(isoquinolin-5-il)urea; (-)1-(6,8-difluoro-3,4-dihidro-espiro-[2H-1-benzopiran-2,1'-ciclobutan]-4-il)-3-(isoquinolin-5-il)urea; (+- )1-(3,4-dihidro-8-difluorometoxi-espiro-[2H-1-benzopiran-2,1'-ciclobutan]-4-il)-3-(isoquinolin-5-il)urea; (+- )1-(6-cloro-3,4-dihidro-espiro-[2H-1-benzopiran-2,1'-ciclobutan]-4-il)-3-(isoquinolin-5-il)urea; (-)1-(6-cloro-3,4-dihidro-espiro-[2H-1-benzopiran-2,1'-ciclobutan]-4-il)-3-(isoquinolin-5-il)urea; (+- )1-(6-bromo-3,4-dihidro-espiro-[2H-1-benzopiran-2,1'-ciclobutan]-4-il)-3-(isoquinolin-5-il)urea; (+- )1-(6,8-dicloro-3,4-dihidro-espiro-[2H-1-benzopiran-2,1'-ciclobutan]-4-il)-3-(isoquinolin-5-il)urea; (+- )1-(6-bromo-3,4-dihidro-7-metilespiro-[2H-1-benzopiran-2,1'-ciclobutan]-4-il)-3-(isoquinolin-5-il)urea; (+- )1-(6,7-dicloro-3,4-dihidro-espiro-[2H-1-benzopiran-2,1'-ciclobutan]-4-il)-3-(isoquinolin-5-il)urea; (+- )1-(6-cloro-3,4-dihidro-7-metilespiro-[2H-1-benzopiran-2,1'-ciclobutan]-4-il)-3-(isoquinolin-5-il)urea; (+- )1-(6-cloro-3,4-dihidro-espiro-[2H-1-benzopiran-2,1'-ciclobutan]-4-il)-3-(8-cloroisoquinolin-5-il)urea; (+- )1-(6-fluoro-3
ARP090103975A 2008-10-17 2009-10-15 Antagonistas del receptor transitorio potencial de vanilloides 1 ( trpv1) utiles para tratar inflamacion y dolor AR073631A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US10636908P 2008-10-17 2008-10-17
US22007509P 2009-06-24 2009-06-24

Publications (1)

Publication Number Publication Date
AR073631A1 true AR073631A1 (es) 2010-11-17

Family

ID=41571121

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP090103975A AR073631A1 (es) 2008-10-17 2009-10-15 Antagonistas del receptor transitorio potencial de vanilloides 1 ( trpv1) utiles para tratar inflamacion y dolor

Country Status (11)

Country Link
US (1) US8604053B2 (es)
EP (1) EP2352726A1 (es)
JP (1) JP2012505907A (es)
CN (1) CN102186836A (es)
AR (1) AR073631A1 (es)
CA (1) CA2737768A1 (es)
MX (1) MX2011004081A (es)
PA (1) PA8845601A1 (es)
TW (1) TW201020236A (es)
UY (1) UY32180A (es)
WO (1) WO2010045401A1 (es)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX2011004090A (es) * 2008-10-17 2011-05-31 Abbott Lab Antagonistas trpv1.
US20100210682A1 (en) * 2009-02-19 2010-08-19 Abbott Laboratories Repeated Dosing of TRPV1 Antagonists
EP2688866A1 (en) * 2011-03-25 2014-01-29 AbbVie Inc. Trpv1 antagonists
US8859584B2 (en) 2011-12-19 2014-10-14 Abbvie, Inc. TRPV1 antagonists
US8969325B2 (en) 2011-12-19 2015-03-03 Abbvie Inc. TRPV1 antagonists
EP2828253A1 (en) * 2012-03-19 2015-01-28 Abide Therapeutics, Inc. Carbamate compounds and of making and using same
JP6115303B2 (ja) * 2012-05-18 2017-04-19 Jnc株式会社 隣接基としてカルボニル基を有するフェノール化合物およびその用途
US8796328B2 (en) 2012-06-20 2014-08-05 Abbvie Inc. TRPV1 antagonists
WO2015179563A2 (en) 2014-05-22 2015-11-26 Abide Therapeutics, Inc. N-hydroxy bicyclic hydantoin carbamates as tools for identification of serine hydrolase targets
US10336709B2 (en) 2015-10-02 2019-07-02 Abide Therapeutics, Inc Lp-PLA2 inhibitors
RU2020105260A (ru) * 2017-07-06 2021-08-06 Дигнити Хелт Новое лечение приливов
CN108929270B (zh) * 2018-08-15 2021-06-08 上海罕道医药科技有限公司 一种药物中间体双取代含氮杂环的胺类化合物的合成
EP3917916A4 (en) 2019-01-30 2022-12-14 Montelino Therapeutics, Inc. Bi-functional compounds and methods for targeted ubiquitination of androgen receptor
PL4019485T3 (pl) 2019-08-23 2024-10-21 Mochida Pharmaceutical Co., Ltd. Sposób wytwarzania pochodnych heterocyklidenoacetamidu
WO2021039023A1 (ja) 2019-08-23 2021-03-04 持田製薬株式会社 ヘテロシクリデンアセトアミド誘導体の製造方法
RU2755206C1 (ru) 2020-05-20 2021-09-14 Федеральное государственное бюджетное учреждение науки Тихоокеанский институт биоорганической химии им. Г.Б. Елякова Дальневосточного отделения Российской академии наук (ТИБОХ ДВО РАН) Средство пролонгированного анальгетического действия и лекарственный препарат на его основе
WO2024102810A1 (en) 2022-11-08 2024-05-16 Montelino Therapeutics, Inc. Bi-functional compounds and methods for targeted ubiquitination of androgen receptor

Family Cites Families (38)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MY115155A (en) 1993-09-09 2003-04-30 Upjohn Co Substituted oxazine and thiazine oxazolidinone antimicrobials.
DE69631347T2 (de) 1995-09-15 2004-10-07 Upjohn Co Aminoaryl oxazolidinone n-oxide
US20030220234A1 (en) * 1998-11-02 2003-11-27 Selvaraj Naicker Deuterated cyclosporine analogs and their use as immunodulating agents
GB9918037D0 (en) * 1999-07-30 1999-09-29 Biochemie Gmbh Organic compounds
GB0206876D0 (en) * 2002-03-22 2002-05-01 Merck Sharp & Dohme Therapeutic agents
GB0226724D0 (en) 2002-11-15 2002-12-24 Merck Sharp & Dohme Therapeutic agents
US7015233B2 (en) * 2003-06-12 2006-03-21 Abbott Laboratories Fused compounds that inhibit vanilloid subtype 1 (VR1) receptor
KR101138216B1 (ko) * 2003-06-12 2012-09-05 아보트 러보러터리즈 바닐로이드 수용체 아형 １(ｖｒ１) 수용체를 억제하는융합 화합물
US7651514B2 (en) * 2003-12-11 2010-01-26 Boston Scientific Scimed, Inc. Nose rider improvement for filter exchange and methods of use
WO2005099353A2 (en) 2004-04-19 2005-10-27 Symed Labs Limited A novel process for the preparation of linezolid and related compounds
WO2006008754A1 (en) 2004-07-20 2006-01-26 Symed Labs Limited Novel intermediates for linezolid and related compounds
JP2008514702A (ja) * 2004-09-29 2008-05-08 エーエムアール テクノロジー インコーポレイテッド 新規シクロスポリン類似体およびそれらの薬学的使用
NZ555318A (en) * 2004-11-24 2011-01-28 Abbott Lab Chromanylurea compounds that inhibit vanilloid receptor subtype 1 (VR1) receptor and uses thereof
TW200716636A (en) * 2005-05-31 2007-05-01 Speedel Experimenta Ag Heterocyclic spiro-compounds
US7514068B2 (en) * 2005-09-14 2009-04-07 Concert Pharmaceuticals Inc. Biphenyl-pyrazolecarboxamide compounds
JP2009511465A (ja) * 2005-10-07 2009-03-19 グレンマーク・ファーマシューティカルズ・エスエー 置換ベンゾ縮合誘導体およびバニロイド受容体リガンドとしてのその使用
CN101365684A (zh) * 2005-10-28 2009-02-11 艾博特公司 抑制trpv1受体的吲唑衍生物
EP2012778A4 (en) 2006-04-18 2011-08-10 Abbott Lab VANILLOID RECEPTOR (VR1) SUBType 1 ANTAGONISTS AND USES THEREOF
US20100029739A1 (en) 2006-10-04 2010-02-04 Uno Jakob Weber Use of a combination of hypothermia inducing drugs
US20090197966A1 (en) 2006-10-04 2009-08-06 Uno Jakob Weber Use of Hypothermia Inducing Drugs
US8796267B2 (en) * 2006-10-23 2014-08-05 Concert Pharmaceuticals, Inc. Oxazolidinone derivatives and methods of use
WO2008059339A2 (en) * 2006-11-13 2008-05-22 Glenmark Pharmaceuticals S.A. Isoquinoline derivatives as vanilloid receptor modulators
CA2672196A1 (en) * 2006-12-20 2008-07-03 Abbott Laboratories Antagonists of the trpv1 receptor and uses thereof
KR101222412B1 (ko) * 2007-02-15 2013-01-15 에프. 호프만-라 로슈 아게 Ｔａａｒ1 리간드로서의 2-아미노옥사졸린
WO2008110863A1 (en) 2007-03-15 2008-09-18 Glenmark Pharmaceuticals S.A. Indazole derivatives and their use as vanilloid receptor ligands
AU2008242703B2 (en) * 2007-04-19 2011-08-18 Concert Pharmaceuticals Inc. Deuterated morpholinyl compounds
US7531685B2 (en) * 2007-06-01 2009-05-12 Protia, Llc Deuterium-enriched oxybutynin
WO2009035598A1 (en) 2007-09-10 2009-03-19 Concert Pharmaceuticals, Inc. Deuterated pirfenidone
US20090118238A1 (en) * 2007-09-17 2009-05-07 Protia, Llc Deuterium-enriched alendronate
US20090088416A1 (en) * 2007-09-26 2009-04-02 Protia, Llc Deuterium-enriched lapaquistat
US20090082471A1 (en) * 2007-09-26 2009-03-26 Protia, Llc Deuterium-enriched fingolimod
WO2009045476A1 (en) * 2007-10-02 2009-04-09 Concert Pharmaceuticals, Inc. Pyrimidinedione derivatives
WO2009051782A1 (en) * 2007-10-18 2009-04-23 Concert Pharmaceuticals Inc. Deuterated etravirine
US20090105338A1 (en) * 2007-10-18 2009-04-23 Protia, Llc Deuterium-enriched gabexate mesylate
PE20091041A1 (es) * 2007-10-19 2009-08-22 Abbott Gmbh & Co Kg Producto de dispersion solida que contiene un compuesto a base de n-aril urea
EP2217548A1 (en) * 2007-10-26 2010-08-18 Concert Pharmaceuticals Inc. Deuterated darunavir
TW200927192A (en) * 2007-11-19 2009-07-01 Alcon Res Ltd Use of TRPV1 receptor antagonists for treating dry eye and ocular pain
MX2011004090A (es) * 2008-10-17 2011-05-31 Abbott Lab Antagonistas trpv1.

Also Published As

Publication number Publication date
US20100137360A1 (en) 2010-06-03
PA8845601A1 (es) 2010-05-26
CA2737768A1 (en) 2010-04-22
EP2352726A1 (en) 2011-08-10
JP2012505907A (ja) 2012-03-08
US8604053B2 (en) 2013-12-10
MX2011004081A (es) 2011-05-31
UY32180A (es) 2010-05-31
WO2010045401A1 (en) 2010-04-22
TW201020236A (en) 2010-06-01
CN102186836A (zh) 2011-09-14

Similar Documents

Publication Publication Date Title
AR073631A1 (es) Antagonistas del receptor transitorio potencial de vanilloides 1 ( trpv1) utiles para tratar inflamacion y dolor
AR061369A1 (es) Derivados de pirimidina y composiciones farmaceuticas que los comprenden
AR061372A1 (es) Amino-imidazoles y sus usos como medicamentos para el tratamiento de mal de alzheimer, demencia y neurodegeneracion
AR045386A1 (es) [1,8] naftiridin-2-onas y compuestos relacionados para el tratamiento de la esquizofrenia
AR061371A1 (es) Amino - imidazolonas y su uso como medicamento para la enfermedad de alzheimer y otras enfermedades neurodegenerativas.
AR061847A1 (es) Derivados de pirimidina 2- amino -5- sustituida. como inhibidores de quinasas. composiciones farmaceuticas.
AR072839A1 (es) Derivados adamantil diamida y usos de los mismos
PE20080841A1 (es) Derivados de quinazolinona e isoquinolinona y su uso para el tratamiento o prevencion de trastornos relacionados con el estres o la depresion
AR043111A1 (es) Derivados monoacilados de o-fenilendiaminas
AR059184A1 (es) Derivados de sulfonamidas, su preparacion y su aplicacion en tarapeutica
AR076550A1 (es) Inhibidores de la janus tirosina kinasa (jak)
ECSP066773A (es) Intermediarios de quinolina como inhibidores de receptores de tirosina quinasas y la síntesis de los mismos
AR054280A1 (es) Derivados de carboxamidas y su empleo en procedimientos de lucha contra enfermedades de plantas y contra hongos nocivos
AR071300A1 (es) Compuestos; composiciones farmaceuticas en base al compuesto y uso del mismo para la manufactura de un medicamento
PE20020735A1 (es) Derivados de quinazolona como antagonistas de receptores adrenergicos alfa-1a/b
AR078786A1 (es) Derivados de la cromenona
PE20021010A1 (es) Derivados espirociclicos como inhibidores de fosfodiesterasa-7
ES2668775T3 (es) Compuestos tetracíclicos
AR042996A1 (es) Un procedimiento de obtencion de derivados de malonamida y medicamentos que los contienen.
AR060050A1 (es) Compuestos moduladores del receptor de s1p y uso de los mismos
AR047538A1 (es) Piridazinonas como antagonistas de las integrinas alfa4
PE20050482A1 (es) Derivados de dihidrobenzofuranilo alcanamida
AR072666A1 (es) Derivados de nip tiazol como inhibidores de la 11-beta-hidroxiesteroide deshidrogenasa-1 (11-b-hsd-1)
AR042827A1 (es) Compuestos de furano condensados
AR080271A2 (es) Proceso para la preparacion de derivados de fenilpropargileter

Legal Events

Date Code Title Description
FA Abandonment or withdrawal