AR072184A1 - Derivados de oxadiazol como agonistas del receptor s1p1 - Google Patents

Derivados de oxadiazol como agonistas del receptor s1p1

Info

Publication number
AR072184A1
AR072184A1 ARP090102219A ARP090102219A AR072184A1 AR 072184 A1 AR072184 A1 AR 072184A1 AR P090102219 A ARP090102219 A AR P090102219A AR P090102219 A ARP090102219 A AR P090102219A AR 072184 A1 AR072184 A1 AR 072184A1
Authority
AR
Argentina
Prior art keywords
alkyl
optionally substituted
halogen
hydrogen
difluoromethoxy
Prior art date
Application number
ARP090102219A
Other languages
English (en)
Original Assignee
Glaxo Group Ltd
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
Priority claimed from GB0811449A external-priority patent/GB0811449D0/en
Priority claimed from GB0909744A external-priority patent/GB0909744D0/en
Application filed by Glaxo Group Ltd filed Critical Glaxo Group Ltd
Publication of AR072184A1 publication Critical patent/AR072184A1/es

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Classifications

    • 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
    • C07D413/04—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
    • 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
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • 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
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • 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
    • A61P37/02—Immunomodulators
    • 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
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Pain & Pain Management (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Rheumatology (AREA)
  • Pulmonology (AREA)
  • Oncology (AREA)
  • Obesity (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Transplantation (AREA)
  • Hospice & Palliative Care (AREA)
  • Communicable Diseases (AREA)
  • Virology (AREA)
  • Psychiatry (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Emergency Medicine (AREA)
  • Dermatology (AREA)

Abstract

La presente se refiere a derivados de oxadiazol que tienen actividad farmacologica, a procesos para su preparacion, a composiciones farmaceuticas que los contienen y a su uso en el tratamiento de diferentes trastornos, en particular trastornos autoinmunes. Reivindicacion 1: Un compuesto de formula (1) o una sal del mismo en la que R5 es como en formula (2) y est  unido en una cualquiera de las posiciones 4, 5, 6 o 7 del grupo indol; A es un fenilo o un anillo heteroarilo de 5 o 6 miembros; R1 es hidrogeno o hasta tres sustituyentes independientemente seleccionados de halogeno, alquilo C1-6, cicloalquilo C3-6, alcoxi C1-6, cicloalquiloxi C3-6, trifluorometoxi, difluorometoxi, trifluorometilo, ciano, nitro, piperidina opcionalmente sustituida, pirrolidina opcionalmente sustituida, fenilo opcionalmente sustituido y anillos heteroar¡licos de 5 o 6 miembros opcionalmente sustituidos; cuando R1 es fenilo, piperidina, pirrolidina o un anillo heteroar¡lico de 5 o 6 miembros, puede estar sustituido con hasta tres sustituyentes seleccionados de halogeno, alquilo C1-6, alcoxi C1-6, trifluorometoxi, difluorometoxi, cicloalquilo C3-6, trifluorometilo y ciano; R2 es hidrogeno o representa hasta tres sustituyentes seleccionados independientemente entre halogeno, alquilo C1-4, alcoxi C1-4, trifluorometoxi, difluorometoxi, trifluorometilo y ciano; uno de R3 y R4 es hidrogeno o alquilo C1-6 y el otro es Z-COOH o alquilo C16-OH; Z est  ausente o es alquilo C1-6 o alquenilo C2-6; cuando Z es alquilo C1-6, est  opcionalmente interrumpido con ciclopropilo, piperidinilo, azetidinilo, pirrolidinilo, N u O y opcionalmente sustituido con O, ciclopropilo, halogeno o metilo, cuando Z es alquenilo C2-6 est  opcionalmente sustituido con metilo, R6 es hidrogeno o alquilo C1-6.
ARP090102219A 2008-06-20 2009-06-18 Derivados de oxadiazol como agonistas del receptor s1p1 AR072184A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GB0811449A GB0811449D0 (en) 2008-06-20 2008-06-20 Compounds
GB0909744A GB0909744D0 (en) 2009-06-05 2009-06-05 Compounds

Publications (1)

Publication Number Publication Date
AR072184A1 true AR072184A1 (es) 2010-08-11

Family

ID=41011874

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP090102219A AR072184A1 (es) 2008-06-20 2009-06-18 Derivados de oxadiazol como agonistas del receptor s1p1

Country Status (7)

Country Link
US (3) US20100029729A1 (es)
EP (1) EP2297139A1 (es)
JP (1) JP2011524880A (es)
AR (1) AR072184A1 (es)
TW (1) TW201011013A (es)
UY (1) UY31922A (es)
WO (1) WO2009153307A1 (es)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2297139A1 (en) * 2008-06-20 2011-03-23 Glaxo Group Limited Compounds
CA2740484C (en) 2008-10-17 2021-09-21 Akaal Pharma Pty Ltd S1p receptors modulators and their use thereof
AU2009304596A1 (en) 2008-10-17 2010-04-22 Akaal Pharma Pty Ltd S1P receptors modulators
GB0910667D0 (en) * 2009-06-19 2009-08-05 Glaxo Wellcome Mfg Pte Ltd Novel compounds
TW201245185A (en) 2011-04-01 2012-11-16 Lundbeck & Co As H New positive allosteric modulators of nicotinic acetylcholine receptor
US8889730B2 (en) 2012-04-10 2014-11-18 Pfizer Inc. Indole and indazole compounds that activate AMPK
KR101567558B1 (ko) * 2012-06-12 2015-11-10 동국대학교 산학협력단 Ｃ형 간염 바이러스의 게놈 복제의 선택적 저해 활성을 갖는 인돌계 화합물, 이의 제조방법 및 이를 유효성분으로 함유하는 ｃ형 간염의 예방 또는 치료용 약학적 조성물
WO2014061676A1 (ja) * 2012-10-16 2014-04-24 武田薬品工業株式会社 複素環化合物
PL2947995T3 (pl) * 2013-01-25 2018-03-30 Compagnie Gervais Danone Proces przygotowania odcedzonego fermentowanego produktu nabiałowego
CA2905242C (en) 2013-03-15 2016-11-29 Pfizer Inc. Indole compounds that activate ampk
US10408748B2 (en) * 2017-01-26 2019-09-10 ClariFruit System and method for evaluating fruits and vegetables
CN106977504A (zh) * 2017-04-06 2017-07-25 济南大学 一种1,2,4‑恶二唑衍生物、制备方法及其医药用途
CN109374575A (zh) * 2018-12-20 2019-02-22 中国烟草总公司郑州烟草研究院 一种基于近红外光谱分析技术的烤烟烟叶底色的鉴别方法
CN109374574A (zh) * 2018-12-20 2019-02-22 中国烟草总公司郑州烟草研究院 一种利用近红外光谱信息鉴别烤烟烟叶蜡质感的方法

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Also Published As

Publication number Publication date
US20100029729A1 (en) 2010-02-04
EP2297139A1 (en) 2011-03-23
US20100010053A1 (en) 2010-01-14
TW201011013A (en) 2010-03-16
UY31922A (es) 2010-01-05
WO2009153307A1 (en) 2009-12-23
JP2011524880A (ja) 2011-09-08
US20110086839A1 (en) 2011-04-14
US8217028B2 (en) 2012-07-10

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