AR078303A1 - Sulfonas sustituidas que modulan selectivamente el receptor cb2 - Google Patents

Sulfonas sustituidas que modulan selectivamente el receptor cb2

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Publication number
AR078303A1
AR078303A1 ARP100103436A ARP100103436A AR078303A1 AR 078303 A1 AR078303 A1 AR 078303A1 AR P100103436 A ARP100103436 A AR P100103436A AR P100103436 A ARP100103436 A AR P100103436A AR 078303 A1 AR078303 A1 AR 078303A1
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AR
Argentina
Prior art keywords
cycloalkyl
hydrogen
ring
membered
alkyl
Prior art date
Application number
ARP100103436A
Other languages
English (en)
Inventor
Robert John Scott
Alessandra Bartolozzi
Doris Riether
Renee Zindell
Patricia Amouzegh
Monika Ermann
Innocent Mushi
Nigel James Blumire
Original Assignee
Boehringer Ingelheim Int
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Publication date
Application filed by Boehringer Ingelheim Int filed Critical Boehringer Ingelheim Int
Publication of AR078303A1 publication Critical patent/AR078303A1/es

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    • 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
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
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    • 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
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    • 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
    • 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
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    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
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    • 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
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    • 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
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/16—Otologicals
    • 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]
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    • A61P35/00—Antineoplastic agents
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    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P9/00—Drugs for disorders of the cardiovascular system
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    • 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
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
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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
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    • 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
    • C07D413/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D413/06—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 carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D417/02—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
    • C07D417/04—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 directly linked by a ring-member-to-ring-member bond
    • 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)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (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)
  • Immunology (AREA)
  • Cardiology (AREA)
  • Pulmonology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Neurology (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Vascular Medicine (AREA)
  • Ophthalmology & Optometry (AREA)
  • Rheumatology (AREA)
  • Transplantation (AREA)
  • Hospice & Palliative Care (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Otolaryngology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Estos 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 la que: Het es un anillo heteroarilo de 5 miembros; R1 es alquilo C1-10, alcoxi C1-10, cicloalquilo C3-10, un anillo heterocíclico saturado de 3-10 miembros, un anillo heteroarilo mono o bicíclico de 5-10 miembros o fenilo, cada uno opcional e independientemente sustituido con 1-3 sustituyentes elegidos entre alquilo C1-4, alcoxi C1-4, cicloalquilo C3-10, alquilsulfonilo C1-4, acilo, oxo, ciano, fenilo, hidroxilo y halogeno; R2 y R3 son alquilo C1-4 o hidrogeno con la condicion de que los dos de R2 y R3 no pueden ser hidrogeno; o R2 y R3 junto con el átomo de carbono al que están unidos forman un anillo heterocíclico o cicloalquilo de 3 a 6 miembros; R4 es hidrogeno o metilo; R5 se elige entre (2) y Ar2, Ar1 es un anillo heteroarilo de 5 miembros o un anillo heterocíclico saturado de 3-10 miembros y Ar2 es un anillo heteroarilo de 5 miembros, cada Ar1 o Ar2 está opcionalmente sustituido independientemente con uno o más R6; R6 es alquilo C1-8, cicloalquilo C3-7 o arilo; cada uno de R7 y R8 es independientemente hidrogeno, cicloalquilo C3-6 o alquilo C1-4 con la condicion de que los dos R7 y R8 no pueden ser hidrogeno; y donde R7 y R8 pueden ciclarse opcionalmente para formar un anillo cicloalquilo C3-7; n es 0, 1 o 2; 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 sal farmacéuticamente aceptable del mismo.
ARP100103436A 2009-09-22 2010-09-21 Sulfonas sustituidas que modulan selectivamente el receptor cb2 AR078303A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US24448209P 2009-09-22 2009-09-22

Publications (1)

Publication Number Publication Date
AR078303A1 true AR078303A1 (es) 2011-10-26

Family

ID=43299636

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP100103436A AR078303A1 (es) 2009-09-22 2010-09-21 Sulfonas sustituidas que modulan selectivamente el receptor cb2

Country Status (6)

Country Link
US (1) US8383651B2 (es)
EP (1) EP2480544A1 (es)
JP (1) JP2013505295A (es)
AR (1) AR078303A1 (es)
TW (1) TW201121962A (es)
WO (1) WO2011037795A1 (es)

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US8629157B2 (en) 2009-01-05 2014-01-14 Boehringer Ingelheim International Gmbh Pyrrolidine compounds which modulate the CB2 receptor
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WO2011088015A1 (en) 2010-01-15 2011-07-21 Boehringer Ingelheim International Gmbh Compounds which modulate the cb2 receptor
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EP2595959B1 (en) 2010-07-22 2015-11-04 Boehringer Ingelheim International GmbH Sulfonyl compounds which modulate the cb2 receptor
JP6262733B2 (ja) 2012-09-04 2018-01-17 シャンハイ ヘンルイ ファーマスーティカル カンパニー リミテッドＳｈａｎｇｈａｉ Ｈｅｎｇｒｕｉ Ｐｈａｒｍａｃｅｕｔｉｃａｌ Ｃｏ．， Ｌｔｄ． イミダゾリン誘導体、その製造法、およびそれらの医薬への適用
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