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AR056043A1 - Agonistas de receptores adrenergicos alfa2c funcionalmente selectivos - Google Patents

Agonistas de receptores adrenergicos alfa2c funcionalmente selectivos

Info

Publication number
AR056043A1
AR056043A1 ARP060103665A ARP060103665A AR056043A1 AR 056043 A1 AR056043 A1 AR 056043A1 AR P060103665 A ARP060103665 A AR P060103665A AR P060103665 A ARP060103665 A AR P060103665A AR 056043 A1 AR056043 A1 AR 056043A1
Authority
AR
Argentina
Prior art keywords
group
heteroaryl
optionally substituted
arylalkyl
alkynyl
Prior art date
Application number
ARP060103665A
Other languages
English (en)
Original Assignee
Schering Corp
Pharmacopeia 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.)
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Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=37401474&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR056043(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Schering Corp, Pharmacopeia Inc filed Critical Schering Corp
Publication of AR056043A1 publication Critical patent/AR056043A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • 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
    • A61P1/12—Antidiarrhoeals
    • 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
    • A61P11/02—Nasal agents, e.g. decongestants
    • 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
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P25/06—Antimigraine agents
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/22—Anxiolytics
    • 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
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • 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
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic 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
    • 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
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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 two hetero rings
    • C07D401/06—Heterocyclic 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 two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/06—Heterocyclic 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

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

Abstract

En sus muchas realizaciones, la presente provee una nueva clase de indolinas como inhibidores de agonistas de receptores adrenérgicos alfa2C; métodos para la preparacion de dichos compuestos; composiciones farmacéuticas que contienen uno o más de dichos compuestos; métodos para la preparacion de formulaciones farmacéuticas que comprenden uno o más de dichos compuestos; y métodos de tratamiento, inhibicion o mejoría de una o más afecciones asociadas con los receptores adrenérgicos alfa2C, empleando dichos compuestos o dichas composiciones farmacéuticas. Reivindicacion 1: Un compuesto representado por la formula (1) estructural, o una sal farmacéuticamente aceptable o un solvato de dicho compuesto, donde: A es un anillo heterocíclico de 5 miembros que contiene 1 a 3 heteroátomos, y está opcionalmente sustituido con por lo menos un R5; J1, J2, y J3 son de modo independiente -N-, -N(O)- o -C(R2)-; J4 es C o N; J5 es -C(R6)- o -N(R6)-; ôlínea simple y línea de puntosö es un enlace simple o doble; R1 se selecciona del grupo que consiste en -(CH2)qYR7, -(CH2)qNR7YR7', -(CH2)qNR7R7', -(CH2)qOYR7, -(CH2)qON=CR7R7', -P(=O)(OR7)(OR7'), -P(=O)(NR7R7')2, y -P(=O)R82; Y se seleccina del grupo que consiste en un enlace, -C(=O)-, - C(=O)NR7-, -C(=O)O-, -C(=NR7)-, -C(=NOR7)-, -C(=NR7)NR7-, -C(=NR7)NR7O-, -S(O)P-, -SO2NR7- , y -C(=S)NR7-; R2 se selecciona de manera independiente del grupo que consiste en H, -OH, halo, -CN, -NO2, -SR7, -NR7R7', -(CH2)qYR7, -(CH2)qNR7YR7, - (CH2)qOYR7, -(CH2)qON=CR7R7', -P(=O)(OR7)(OR7'), -P(=O)NR7R7', y -P(=O)R82, y grupos alquilo, alcoxi, alquenilo, alqueniloxi, alquinilo, cicloalquilo, cicloalcoxi, arilo, ariloxi, arilalquilo, heteroarilo, heteroarilalquilo, heterociclilo, y heterociclilalquilo, opcionalmente sustituidos con por lo menos un R5; R3 se selecciona de manera independiente del grupo que consiste en H y (=O), y grupos alquilo, alcoxi, alquenilo, alqueniloxi, alquinilo, cicloalquilo, cicloalcoxi, arilo, ariloxi, arilalquilo, heteroarilo, heteroarilalquilo, heterociclilo, y heterociclilalquilo, opcionalmente sustituidos con por lo menos un R5, siempre que cuando w es 3, no más de 2 de los grupos R3 pueden ser (=O); R4 se selecciona de manera independiente del grupo que consiste en H y -CN, y grupos alquilo, alcoxi, alquenilo, alqueniloxi, alquinilo, cicloalquilo, cicloalcoxi, arilo, ariloxi, arilalquilo, heteroarilo, heteroarilalquilo, heterociclilo, y heterociclilalquilo, opcionalmente sustituidos con por lo menos un R5; R5 se selecciona de manera independiente del grupo que consiste en H, halo, -OH, -CN, -NO2, -NR7R7', y -SR7, y grupos alquilo, alcoxi, alquenilo, alqueniloxi, alquinilo, cicloalquilo, cicloalcoxi, arilo, ariloxi, arilalquilo, heteroarilo, heteroarilalquilo, heterociclilo, y heterociclilalquilo, donde cada uno está opcionalmente sustituido con por lo menos uno de los sustituyentes halo, -OH, -CN, -NO2, -NR7R7', y -S(O)pR7; R6 se selecciona de manera independiente del grupo que consiste en H y grupos alquilo, alcoxi, alquenilo, alqueniloxi, alquinilo, cicloalquilo, cicloalcoxi, arilo, ariloxi, arilalquilo, heteroarilo, heteroarilalquilo, heterociclilo, y heterociclilalquilo, donde cada uno está opcionalmente sustituido con por lo menos uno de los sustituyentes halo, -OH, -CN, -NO2, -NR7R7', y -SR7, y -C(=O)R7, -C(=O)OR7, -C(=O)NR7R7', -SO2R8 y -SO2NR7R7'; R7 se selecciona de manera independiente del grupo que consiste en H y grupos alquilo, alquenilo, alquinilo, cicloalquilo, arilo, arilalquilo, heterociclilo, heteroarilo, y heteroarilalquilo, donde cada uno está opcionalmente sustituido con por lo menos uno de los sustituyentes halo, alcoxi, -OH, -CN, -NO2, -N(R11)2 y - S(O)pR11; R7' se selecciona de manera independiente del grupo que consiste en H y grupos alquilo, alquenilo, alquinilo, cicloalquilo, arilo, arilalquilo, heteroarilo, y heteroarilalquilo, donde cada uno está opcionalmente sustituido con por lo menos uno de los sustituyentes halo, -OH, -CN, -NO2, -N(R11)2, y -SR11; o R7 y R7' junto con el átomo de nitrogeno al cual están unidos forman un anillo de 3 a 8 miembros heterociclilo, heterociclenilo o heteroarilo, que tiene, además del átomo N, 1 o 2 heteroátomos adicionales seleccionados del grupo que consiste en O, N, -N(R9)- y S, donde dichos anillos están opcionalmente sustituidos con 1 a 5 porciones R5 seleccionados en forma independiente; R8 se selecciona de manera independiente del grupo que consiste en grupos alquilo, alquenilo, alquinilo, cicloalquilo, arilo, arilalquilo, heterociclilo, heteroarilo, y heteroarilalquilo, donde cada uno está opcionalmente sustituido con por lo menos uno de los sustituyentes halo, alcoxi, -OH, -CN, - NO2, -N(R11)2, y -SR11; R9 se selecciona de manera independiente del grupo que consiste en H, -C(O)-R10, -C(O)-OR10, y -S(O)p-OR10 y grupos alquilo, alquenilo, alquinilo, cicloalquilo, arilo, arilalquilo, heteroarilo, y heteroarilalquilo donde cada uno está opcionalmente sustituido con por lo menos uno de los sustituyentes halo, -OH, -CN, -NO2, -N(R11)2, y -SR11; y R10 se selecciona del grupo que consiste en grupos alquilo, alquenilo, alquinilo, cicloalquilo, arilo, arilalquilo, heteroarilo, y heteroarilalquilo, donde cada uno está opcionalmente sustituido con por lo menos uno de los sustituyentes halo, -OH, -CN, -NO2, -N(R11)2 y -SR11; R11 es una porcion seleccionada de modo independiente del grupo que consiste en H y alquilo, alcoxi, alquenilo, alqueniloxi, alquinilo, cicloalquilo, cicloalcoxi, arilo, ariloxi, arilalquilo, heteroarilo, heteroarilalquilo, heterociclilo, y heterociclilalquilo; m es 1-5; n es 1 -3; p es 0-2; q es 0-6; y w es 1-3; con las siguientes condiciones: a) si J1-J3 son -C(H)-, R1 es -(CH2)qOYR7, q es 0, y A es imidazolilo no sustituido, entonces Y no es un enlace; b) si J1-J3 son -C(H)-, R1 es -(CH2)qYR7, q es 0, y A es imidazolilo no sustituido, entonces Y no es un enlace; c) si J4 es N, entonces J5 es -C(R6)-; y d) si J4 es C, entonces J5 es -N(R6)-.
ARP060103665A 2005-08-25 2006-08-23 Agonistas de receptores adrenergicos alfa2c funcionalmente selectivos AR056043A1 (es)

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US (1) US7803828B2 (es)
EP (1) EP1945626B1 (es)
JP (1) JP2009506047A (es)
KR (1) KR20080039982A (es)
CN (1) CN101296920A (es)
AR (1) AR056043A1 (es)
AT (1) ATE517883T1 (es)
AU (1) AU2006283104A1 (es)
BR (1) BRPI0615307A2 (es)
CA (1) CA2620171A1 (es)
EC (1) ECSP088222A (es)
IL (1) IL189679A0 (es)
NO (1) NO20081426L (es)
PE (1) PE20070336A1 (es)
RU (1) RU2008110908A (es)
SG (1) SG165314A1 (es)
TW (1) TWI316515B (es)
WO (1) WO2007024944A1 (es)
ZA (1) ZA200802453B (es)

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