AR077362A1 - Compuestos que modulan selectivamente el receptor cb2 - Google Patents

Compuestos que modulan selectivamente el receptor cb2

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Publication number
AR077362A1
AR077362A1 ARP100102105A ARP100102105A AR077362A1 AR 077362 A1 AR077362 A1 AR 077362A1 AR P100102105 A ARP100102105 A AR P100102105A AR P100102105 A ARP100102105 A AR P100102105A AR 077362 A1 AR077362 A1 AR 077362A1
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AR
Argentina
Prior art keywords
alkyl
cycloalkyl
ring
optionally
hydrogen
Prior art date
Application number
ARP100102105A
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English (en)
Inventor
Alessandra Bartolozzi
Eugene Richard Hickey
Doris Riether
Lifen Wu
Renee Zindell
Przemyslaw Zawadzki
Edward Thomas Glenn
Nigel Blumire
Monika Ermann
Someina Khor
Original Assignee
Boehringer Ingelheim Int
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Application filed by Boehringer Ingelheim Int filed Critical Boehringer Ingelheim Int
Publication of AR077362A1 publication Critical patent/AR077362A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • 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
    • A61K31/42—Oxazoles
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
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    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
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    • 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
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • 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
    • C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
    • C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
    • C07D261/06—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
    • C07D261/10—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more 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
    • C07D261/14—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
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    • C07D417/00—Heterocyclic 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
    • C07D417/02—Heterocyclic 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 two hetero rings
    • C07D417/06—Heterocyclic 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 two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
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    • C07D—HETEROCYCLIC COMPOUNDS
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    • C07D417/02—Heterocyclic 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 two hetero rings
    • C07D417/12—Heterocyclic 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 two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/14—Heterocyclic 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

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  • Health & Medical Sciences (AREA)
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  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Immunology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Neurology (AREA)
  • Pulmonology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Rheumatology (AREA)
  • Diabetes (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Endocrinology (AREA)
  • Otolaryngology (AREA)
  • Hospice & Palliative Care (AREA)
  • Ophthalmology & Optometry (AREA)
  • Transplantation (AREA)
  • Vascular Medicine (AREA)
  • Dermatology (AREA)
  • Hematology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Abstract

Los compuestos se unen a y son agonistas, antagonistas o agonistas inversos del receptor CB2, y son utiles para tratar la inflamacion. Los compuestos que son agonistas también son utiles para tratar el dolor. Reivindicacion 1: Un compuesto caracterizado porque tiene la formula (1), en donde: anillo A es un anillo heteroarilo de 5 miembros; R1 es hidrogeno, alquilo C1-10 o cicloalquilo C3-10, que está opcionalmente sustituido con 1 - 3 alquilo C1-10, cada R1 o sus sustituyente está opcionalmente halogenado; R2 es alquilo C1-10, cicloalquilo C3-10, arilsulfonilo, arilcarbonilo, acilo C1-10, cicloalquil C3-10-carbonilo, heterociclilcarbonilo, heteroarilcarbonilo, heterociclilo, bencilo, fenetilo, arilo o heteroarilo y cada uno opcionalmente sustituido independientemente con 1 a 3 sustituyentes elegidos entre alquilo C1-6, cicloalquilo C3-10, alcoxi C1-6, alquiltio C1-6, alquil C1-6-sulfonilo, alcoxi C1-6-carbonilo, alquil C1-6-amino, cicloalquil C3-6-amino, dialquil C1-6-amino, alquil C1-6-aminocarbonilo, acil C1-6-amino, dialquil C1-6-aminocarbonilo, hidroxilo, halogeno, ciano, nitro, oxo, heterociclilo, arilo y heteroarilo, cada sustituyente sobre R2, cuando sea posible, está opcionalmente halogenado o sustituido con 1 a 3 grupos alquilo C1-6, acilo C1-6, alquilsulfonilo C1-6, ciano, arilo, oxo o hidroxilo; o R1 y R2, junto con el átomo de nitrogeno al que están unidos, forman un heterociclo monocíclico, bicíclico o espirocíclico o un anillo heteroarilo monocíclico o bicíclico, cada uno opcionalmente sustituido con 1 a 3 grupos alquilo C1-6, alcoxi C1-6, acilo C1-6, alquil C1-6-sulfonilo, ciano, arilo, oxo, hidroxilo o halogeno, estando cada sustituyente del anillo opcionalmente halogenado adicionalmente cuando sea posible; R3 y R3' son independientemente hidrogeno o alquilo C1-6 opcionalmente halogenado, con la condicion de que R3 y R3' no puedan ser simultáneamente hidrogeno; o R3 y R3', junto con el átomo de carbono al que están unidos, forman un anillo cicloalquilo o heterocíclico de 3 a 6 miembros, cada uno opcionalmente halogenado; R4 es hidrogeno o metilo; R5 se elige entre los restos del grupo de formulas (2); m es 0, 1, 2 o 3; R6 es hidrogeno, alquilo C1-4 o alcoxi C1-4; R7 y R8 son, cada uno independientemente, hidrogeno o alquilo C1-4, con la condicion de que tanto R7 como R8 no puedan ser hidrogeno; y en donde R7 y R8 pueden ciclarse opcionalmente para formar un anillo cicloalquilo C3-7; R9 es alquilo C1-6 o arilo; anillo B es un anillo heterocíclico de 5 - 6 miembros; n es 0, 1 o 2; en donde cualquier átomo de carbono de la formula (1) o cualquier sustituyente R indicado anteriormente está opcionalmente halogenado parcial o totalmente cuando sea posible; o una de sus sales farmacéuticamente aceptable.
ARP100102105A 2009-06-15 2010-06-14 Compuestos que modulan selectivamente el receptor cb2 AR077362A1 (es)

Applications Claiming Priority (1)

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US18692009P 2009-06-15 2009-06-15

Publications (1)

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AR077362A1 true AR077362A1 (es) 2011-08-24

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Country Status (23)

Country Link
US (2) US8299103B2 (es)
EP (2) EP2443100A2 (es)
JP (1) JP5492297B2 (es)
KR (1) KR20120047211A (es)
CN (1) CN102803235A (es)
AP (1) AP2011005988A0 (es)
AR (1) AR077362A1 (es)
AU (1) AU2010260397A1 (es)
BR (1) BRPI1011668A2 (es)
CA (1) CA2765525A1 (es)
CL (1) CL2011003160A1 (es)
CO (1) CO6470896A2 (es)
EA (1) EA201200019A1 (es)
EC (1) ECSP12011583A (es)
IL (1) IL216348A0 (es)
MA (1) MA33362B1 (es)
MX (1) MX2011013152A (es)
PE (1) PE20120561A1 (es)
SG (1) SG176864A1 (es)
TN (1) TN2011000639A1 (es)
TW (1) TW201111374A (es)
WO (1) WO2010147792A2 (es)
ZA (1) ZA201108258B (es)

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KR20090069318A (ko) 2006-09-25 2009-06-30 베링거 인겔하임 인터내셔날 게엠베하 Ｃｂ2 수용체를 조절하는 화합물
WO2008048914A1 (en) 2006-10-17 2008-04-24 Boehringer Ingelheim International Gmbh Polycyclic compounds which modulate the cb2 receptor
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EP2217565B1 (en) * 2007-11-07 2013-05-22 Boehringer Ingelheim International GmbH Compounds which modulate the cb2 receptor
EP2265585B1 (en) * 2008-02-21 2014-09-17 Boehringer Ingelheim International GmbH Amine and ether compounds which modulate the cb2 receptor
JP5749162B2 (ja) * 2008-07-10 2015-07-15 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Ｃｂ２受容体を調節するスルホン化合物
KR20110063438A (ko) * 2008-09-25 2011-06-10 베링거 인겔하임 인터내셔날 게엠베하 Ｃｂ2 수용체를 선택적으로 조절하는 설포닐 화합물
EP2384320B1 (en) 2009-01-05 2015-03-04 Boehringer Ingelheim International GmbH Pyrrolidine compounds which modulate the cb2 receptor
WO2010096371A2 (en) 2009-02-18 2010-08-26 Boehringer Ingelheim International Gmbh Heterocyclic compounds which modulate the cb2 receptor
US8299103B2 (en) 2009-06-15 2012-10-30 Boehringer Ingelheim International Gmbh Compounds which selectively modulate the CB2 receptor
PL2442870T3 (pl) 2009-06-15 2014-12-31 Takeda Pharmaceuticals Co Pochodne pirazynooksazepiny
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