CA2524867A1 - 3-(2-amino-1-azacyclyl)-5-aryl-1,2,4-oxadiazoles as s1p receptor agonists - Google Patents

3-(2-amino-1-azacyclyl)-5-aryl-1,2,4-oxadiazoles as s1p receptor agonists Download PDF

Info

Publication number
CA2524867A1
CA2524867A1 CA002524867A CA2524867A CA2524867A1 CA 2524867 A1 CA2524867 A1 CA 2524867A1 CA 002524867 A CA002524867 A CA 002524867A CA 2524867 A CA2524867 A CA 2524867A CA 2524867 A1 CA2524867 A1 CA 2524867A1
Authority
CA
Canada
Prior art keywords
disease
group
mhz
halo
compound according
Prior art date
Legal status (The legal status 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 status listed.)
Abandoned
Application number
CA002524867A
Other languages
English (en)
French (fr)
Inventor
Vincent J. Colandrea
George A. Doherty
Jeffrey J. Hale
Christopher Lynch
Sander G. Mills
William Edward Neway, Iii
Leslie Toth
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck and Co Inc
Original Assignee
Individual
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 Individual filed Critical Individual
Publication of CA2524867A1 publication Critical patent/CA2524867A1/en
Abandoned legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/04Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/14Drugs for dermatological disorders for baldness or alopecia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • A61P27/12Ophthalmic agents for cataracts
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/20Antivirals for DNA viruses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06Antianaemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D271/00Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
    • C07D271/02Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
    • C07D271/061,2,4-Oxadiazoles; Hydrogenated 1,2,4-oxadiazoles
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic 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)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Virology (AREA)
  • Diabetes (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Pulmonology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Dermatology (AREA)
  • Hematology (AREA)
  • Neurology (AREA)
  • Molecular Biology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Ophthalmology & Optometry (AREA)
  • Obesity (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Hospice & Palliative Care (AREA)
  • Urology & Nephrology (AREA)
  • Endocrinology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • AIDS & HIV (AREA)
CA002524867A 2003-05-15 2004-05-12 3-(2-amino-1-azacyclyl)-5-aryl-1,2,4-oxadiazoles as s1p receptor agonists Abandoned CA2524867A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US47065903P 2003-05-15 2003-05-15
US60/470,659 2003-05-15
PCT/US2004/014837 WO2004103279A2 (en) 2003-05-15 2004-05-12 3-(2-amino-1-azacyclyl)-5-aryl-1,2,4-oxadiazoles as s1p receptor agonists

Publications (1)

Publication Number Publication Date
CA2524867A1 true CA2524867A1 (en) 2004-12-02

Family

ID=33476733

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002524867A Abandoned CA2524867A1 (en) 2003-05-15 2004-05-12 3-(2-amino-1-azacyclyl)-5-aryl-1,2,4-oxadiazoles as s1p receptor agonists

Country Status (7)

Country Link
US (1) US20060252741A1 (enExample)
EP (1) EP1625123A4 (enExample)
JP (1) JP2006528980A (enExample)
CN (1) CN1788008A (enExample)
AU (1) AU2004240586A1 (enExample)
CA (1) CA2524867A1 (enExample)
WO (1) WO2004103279A2 (enExample)

Families Citing this family (116)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2003259296A1 (en) 2002-07-30 2004-02-16 University Of Virginia Patent Foundation Compounds active in spinigosine 1-phosphate signaling
WO2005041899A2 (en) 2003-11-03 2005-05-12 University Of Virginia Patent Foundation Orally available sphingosine 1-phosphate receptor agonists and antagonists
AU2004299456B2 (en) * 2003-12-17 2010-10-07 Merck Sharp & Dohme Corp. (3,4-disubstituted)propanoic carboxylates as S1P (Edg) receptor agonists
PL1772145T3 (pl) 2004-07-16 2011-08-31 Kyorin Seiyaku Kk Sposób skutecznego stosowania leku i sposób dotyczący zapobiegania efektom ubocznym
WO2006010379A1 (en) 2004-07-29 2006-02-02 Actelion Pharmaceuticals Ltd. Novel thiophene derivatives as immunosuppressive agents
RU2383536C2 (ru) 2004-08-04 2010-03-10 Тайсо Фармасьютикал Ко., Лтд. Производное триазола
US20060223866A1 (en) * 2004-08-13 2006-10-05 Praecis Pharmaceuticals, Inc. Methods and compositions for modulating sphingosine-1-phosphate (S1P) receptor activity
BRPI0514316A (pt) 2004-08-13 2008-06-10 Praecis Pharm Inc métodos e composições para modulação de atividade de receptor de esfingosina-1-fosfato (s1p)
RU2376285C2 (ru) * 2004-10-12 2009-12-20 Киорин Фармасьютикал Ко., Лтд. Процесс получения гидрохлорида 2-амино-2-[2-[4-(3-бензилоксифенилтио)-2-хлорфенилэтил]-1,3-пропандиола] и его гидратов, а также промежуточные продукты их получения
BRPI0607435A2 (pt) 2005-02-14 2010-04-06 Univ Virginia composto ou um sal ou éster farmaceuticamente aceitável do mesmo, e, uso de um composto
ATE413874T1 (de) * 2005-03-23 2008-11-15 Actelion Pharmaceuticals Ltd Neue thiophen-derivate als sphingosin-1-phosphat- 1-rezeptorantagonisten
WO2006100631A1 (en) 2005-03-23 2006-09-28 Actelion Pharmaceuticals Ltd Hydrogenated benzo (c) thiophene derivatives as immunomodulators
WO2006114400A1 (en) 2005-04-26 2006-11-02 Neurosearch A/S Novel oxadiazole derivatives and their medical use
WO2006131336A1 (en) * 2005-06-08 2006-12-14 Novartis Ag POLYCYCLIC OXADIAZOLES OR I SOXAZOLES AND THEIR USE AS SlP RECEPTOR LIGANDS
DK1932522T3 (da) * 2005-10-07 2012-07-02 Kyorin Seiyaku Kk Terapeutisk middel mod leversygdom indeholdende 2-amino-1,3-propandiolderivat som aktiv bestanddel
TWI404706B (zh) 2006-01-11 2013-08-11 Actelion Pharmaceuticals Ltd 新穎噻吩衍生物
KR20080092385A (ko) 2006-01-24 2008-10-15 액테리온 파마슈티칼 리미티드 신규한 피리딘 유도체
JP2009528274A (ja) 2006-01-27 2009-08-06 ユニバーシティ オブ バージニア パテント ファンデーション 神経因性疼痛の治療法
GB0601744D0 (en) 2006-01-27 2006-03-08 Novartis Ag Organic compounds
EP1988083B1 (en) 2006-02-03 2014-04-02 Taisho Pharmaceutical Co., Ltd. Triazole derivative
TWI389683B (zh) * 2006-02-06 2013-03-21 Kyorin Seiyaku Kk A therapeutic agent for an inflammatory bowel disease or an inflammatory bowel disease treatment using a 2-amino-1,3-propanediol derivative as an active ingredient
US7994204B2 (en) 2006-02-06 2011-08-09 Taisho Pharmaceutical Co., Ltd Binding inhibitor of sphingosine-1-phosphate
EP1987013A1 (en) 2006-02-09 2008-11-05 University Of Virginia Patent Foundation Bicyclic sphingosine 1-phosphate analogs
KR20080096780A (ko) * 2006-02-21 2008-11-03 유니버시티 오브 버지니아 페이턴트 파운데이션 S1p 수용체 효능제로서의 페닐-시클로알킬 및 페닐-헤테로시클릭 유도체
JP5099005B2 (ja) 2006-04-03 2012-12-12 アステラス製薬株式会社 ヘテロ化合物
CN101501049B (zh) 2006-08-08 2013-04-24 杏林制药株式会社 氨基磷酸酯衍生物以及将它们作为有效成分的s1p受体调节剂
RU2458044C2 (ru) * 2006-08-08 2012-08-10 Киорин Фармасьютикал Ко., Лтд. Производное аминоспирта и иммунодепрессивное средство, содержащее его в качестве активного ингредиента
TWI408139B (zh) 2006-09-07 2013-09-11 Actelion Pharmaceuticals Ltd 新穎噻吩衍生物
PL2069336T3 (pl) 2006-09-07 2013-05-31 Idorsia Pharmaceuticals Ltd Pochodne pirydyn-4-ylu jako środki immunomodulujące
AU2007292992B2 (en) 2006-09-08 2013-01-10 Actelion Pharmaceuticals Ltd Pyridin-3-yl derivatives as immunomodulating agents
ES2393412T3 (es) * 2006-09-21 2012-12-21 Actelion Pharmaceuticals Ltd. Derivados de fenilo y su uso como inmunomoduladores
WO2008064337A2 (en) 2006-11-21 2008-05-29 University Of Virginia Patent Foundation Benzocycloheptyl analogs having sphingosine 1-phosphate receptor activity
EP2099741A2 (en) 2006-11-21 2009-09-16 University Of Virginia Patent Foundation Hydrindane analogs having sphingosine 1-phosphate receptor agonist activity
EP2097397A1 (en) 2006-11-21 2009-09-09 University Of Virginia Patent Foundation Tetralin analogs having sphingosine 1-phosphate agonist activity
JO2701B1 (en) 2006-12-21 2013-03-03 جلاكسو جروب ليميتد Vehicles
GB0625648D0 (en) * 2006-12-21 2007-01-31 Glaxo Group Ltd Compounds
GB0625647D0 (en) * 2006-12-21 2007-01-31 Glaxo Group Ltd Compounds
AU2013201157B2 (en) * 2006-12-21 2015-06-11 Glaxo Group Limited Indole derivatives as s1p1 receptor agonists
CN100494178C (zh) * 2007-02-02 2009-06-03 广东东阳光药业有限公司 一种吡啶甲脒及其盐的制备方法
EP2129218B1 (en) * 2007-02-16 2016-10-19 Emisphere Technologies, Inc. Compounds having a cyclic moiety and compositions for delivering active agents
SI2125797T1 (sl) * 2007-03-16 2014-03-31 Actelion Pharmaceuticals Ltd. Derivati amino-piridina kot agonisti receptorja s1p1/edg1
DE602008005285D1 (de) * 2007-04-19 2011-04-14 Glaxo Group Ltd Oxadiazolsubstituierte indazolderivate zur verwendung als sphingosin-1-phosphat (s1p) -agonisten
AU2008282156B2 (en) * 2007-07-31 2014-07-17 Vertex Pharmaceuticals Incorporated Process for preparing 5-fluoro-1H-pyrazolo [3, 4-b] pyridin-3-amine and derivatives thereof
SI2177512T1 (sl) 2007-08-01 2012-06-29 Taisho Pharmaceutical Co Ltd Inhibitor vezave S1P1
ES2361463T3 (es) * 2007-08-17 2011-06-17 Actelion Pharmaceuticals Ltd. Derivados de piridina como moduladores del receptor s1p1/edg1.
EP2193125B1 (en) * 2007-10-04 2017-01-11 Merck Serono S.A. Oxadiazole derivatives
MX2010003614A (es) * 2007-10-04 2010-04-21 Merck Serono Sa Compuestos de diarilo oxadiazol.
EP2217594B1 (en) * 2007-11-01 2014-01-08 Actelion Pharmaceuticals Ltd. Novel pyrimidine derivatives
TW200946105A (en) 2008-02-07 2009-11-16 Kyorin Seiyaku Kk Therapeutic agent or preventive agent for inflammatory bowel disease containing amino alcohol derivative as active ingredient
CA2714665A1 (en) * 2008-03-06 2009-09-11 Actelion Pharmaceuticals Ltd Pyridine compounds
GB0807910D0 (en) 2008-04-30 2008-06-04 Glaxo Group Ltd Compounds
BRPI0915052A2 (pt) 2008-05-08 2019-09-24 Allergan Inc compostos de 1,7-difenil-1,2,3,5,6,7-hexa-hidropirido [3,2,1-ij] quinolina substituído terapeuticamente úteis
WO2009151621A1 (en) * 2008-06-13 2009-12-17 Arena Pharmaceuticals, Inc. Substituted (1, 2, 4-0xadiaz0l-3-yl) indolin-1-yl carboxylic acid derivatives useful as s1p1 agonists
WO2009151626A1 (en) * 2008-06-13 2009-12-17 Arena Pharmaceuticals, Inc. Substituted (1, 2, 4-0xadiaz0l-3-yl) indolin-1-yl carboxylic acid derivatives useful as s1p1 agonists
US8580841B2 (en) 2008-07-23 2013-11-12 Arena Pharmaceuticals, Inc. Substituted 1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid derivatives useful in the treatment of autoimmune and inflammatory disorders
EP2342205B1 (en) 2008-08-27 2016-04-20 Arena Pharmaceuticals, Inc. Substituted tricyclic acid derivatives as s1p1 receptor agonists useful in the treatment of autoimmune and inflammatory disorders
EP2370424A1 (en) 2008-11-10 2011-10-05 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
EP2376485B1 (en) 2008-12-19 2017-12-06 Vertex Pharmaceuticals Incorporated Pyrazine derivatives useful as inhibitors of atr kinase
EP2210890A1 (en) * 2009-01-19 2010-07-28 Almirall, S.A. Oxadiazole derivatives as S1P1 receptor agonists
WO2010085581A1 (en) * 2009-01-23 2010-07-29 Bristol-Myers Squibb Company Substituted oxadiazole derivatives as s1p agonists in the treatment of autoimmune and inflammatory diseases
ES2405054T3 (es) * 2009-01-23 2013-05-30 Bristol-Myers Squibb Company Derivados de pirazol-1,2,4-oxadiazol como agonistas de esfingosina-1-fosfato
AR075781A1 (es) * 2009-03-03 2011-04-27 Merck Serono Sa Derivados de oxadiazol piridina como agonistas del receptor s1p1/edg1 y un metodo para su preparacion.
WO2011007324A1 (en) * 2009-07-16 2011-01-20 Actelion Pharmaceuticals Ltd Pyridin-4-yl derivatives
US8399451B2 (en) 2009-08-07 2013-03-19 Bristol-Myers Squibb Company Heterocyclic compounds
EP4148045A1 (en) 2010-01-27 2023-03-15 Arena Pharmaceuticals, Inc. Intermediate compounds for the preparation of (r)-2-(7-(4-cyclopentyl-3- (trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[b] indol-3-yl)acetic acid and salts thereof
ES2558087T3 (es) 2010-03-03 2016-02-01 Arena Pharmaceuticals, Inc. Procesos para la preparación de moduladores del receptor S1P1 y formas cristalinas de los mismos
US8247436B2 (en) 2010-03-19 2012-08-21 Novartis Ag Pyridine and pyrazine derivative for the treatment of CF
WO2011133734A1 (en) 2010-04-23 2011-10-27 Bristol-Myers Squibb Company 4 - (5 - isoxazolyl or 5 - pyrrazolyl -1,2,4- oxadiazol - 3 - yl) -mandelic acid amides as sphingosin- 1 - phosphate 1 rreceptor agonists
EP2569286B1 (en) 2010-05-12 2014-08-20 Vertex Pharmaceuticals Inc. Compounds useful as inhibitors of atr kinase
WO2011143399A1 (en) 2010-05-12 2011-11-17 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
US8962631B2 (en) 2010-05-12 2015-02-24 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
EP2569284B1 (en) 2010-05-12 2015-07-08 Vertex Pharmaceuticals Incorporated 2-aminopyridine derivatives useful as inhibitors of atr kinase
KR20130066633A (ko) 2010-05-12 2013-06-20 버텍스 파마슈티칼스 인코포레이티드 Atr 키나제의 억제제로서 유용한 화합물
JP2013526540A (ja) 2010-05-12 2013-06-24 バーテックス ファーマシューティカルズ インコーポレイテッド Atrキナーゼ阻害剤として有用な化合物
WO2011163527A1 (en) 2010-06-23 2011-12-29 Vertex Pharmaceuticals Incorporated Pyrrolo- pyrazine derivatives useful as inhibitors of atr kinase
US9187437B2 (en) 2010-09-24 2015-11-17 Bristol-Myers Squibb Company Substituted oxadiazole compounds
ES2525298T3 (es) * 2010-11-03 2014-12-19 Bristol-Myers Squibb Company Compuestos heterocíclicos como agonistas del S1P1 para el tratamiento de enfermedades autoinmunes y vasculares
AU2011337004A1 (en) 2010-12-03 2013-07-11 Allergan, Inc. Novel phenyl oxadiazole derivatives as sphingosine 1-phosphate (S1P) receptor modulators
JP2013544831A (ja) 2010-12-03 2013-12-19 アラーガン インコーポレイテッド スフィンゴシン−1−リン酸(s1p)受容体モジュレーターとしての新規アゼチジン誘導体
JP2013544832A (ja) * 2010-12-03 2013-12-19 アラーガン インコーポレイテッド スフィンゴシン−1−リン酸(s1p)受容体モジュレーターとしての新規オキサジアゾール誘導体
FR2968556B1 (fr) * 2010-12-13 2013-12-27 Centre Nat Rech Scient Inhibiteurs des infections a vih et leurs utilisations
UA109804C2 (xx) 2011-01-19 2015-10-12 2-метоксипіридин-4-ільні похідні
WO2012138938A1 (en) 2011-04-05 2012-10-11 Vertex Pharmaceuticals Incorporated Aminopyrazine compounds useful as inhibitors of tra kinase
US8822469B2 (en) 2011-06-22 2014-09-02 Vertex Pharmaceuticals Incorporated Pyrrolo[2,3-B]pyrazines useful as inhibitors of ATR kinase
US9096602B2 (en) 2011-06-22 2015-08-04 Vertex Pharmaceuticals Incorporated Substituted pyrrolo[2,3-B]pyrazines as ATR kinase inhibitors
US9309250B2 (en) 2011-06-22 2016-04-12 Vertex Pharmaceuticals Incorporated Substituted pyrrolo[2,3-b]pyrazines as ATR kinase inhibitors
US8853217B2 (en) 2011-09-30 2014-10-07 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
BR112014007690B1 (pt) 2011-09-30 2022-10-04 Vertex Pharmaceuticals Incorporated Usos de inibidores de atr no tratamento de câncer pancreático e câncer de pulmão de células não pequenas
CN103987709B (zh) 2011-09-30 2016-09-28 沃泰克斯药物股份有限公司 用于制备可用作atr激酶抑制剂的化合物的方法
IN2014KN00943A (enExample) 2011-09-30 2015-08-21 Vertex Pharma
EP2751088B1 (en) 2011-09-30 2016-04-13 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
WO2013071093A1 (en) 2011-11-09 2013-05-16 Vertex Pharmaceuticals Incorporated Pyrazine compounds useful as inhibitors of atr kinase
US8846917B2 (en) 2011-11-09 2014-09-30 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
US8841449B2 (en) 2011-11-09 2014-09-23 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
WO2013071094A1 (en) 2011-11-09 2013-05-16 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
WO2013071090A1 (en) 2011-11-09 2013-05-16 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
EP3311816A1 (en) 2012-04-05 2018-04-25 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase for the treatment of cancer
US8999632B2 (en) 2012-10-04 2015-04-07 Vertex Pharmaceuticals Incorporated Method for measuring ATR inhibition mediated increases in DNA damage
EP2909202A1 (en) 2012-10-16 2015-08-26 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
US8735433B1 (en) 2012-11-14 2014-05-27 Allergan, Inc. Aryl oxadiazole derivatives as sphingosine 1-phosphate (S1P) receptor modulators
PL3808749T3 (pl) 2012-12-07 2023-07-10 Vertex Pharmaceuticals Incorporated Pirazolo[1,5-a]pirymidyny użyteczne jako inhibitory kinazy atr do leczenia chorób nowotworowych
US8871755B2 (en) 2013-02-12 2014-10-28 Allergan, Inc. Alkene azetidine derivatives as sphingosine 1-phosphate (S1P) receptor modulators
JP2016512815A (ja) 2013-03-15 2016-05-09 バーテックス ファーマシューティカルズ インコーポレイテッドVertex Pharmaceuticals Incorporated Atrキナーゼの阻害剤として有用な縮合ピラゾロピリミジン誘導体
PL3077397T3 (pl) 2013-12-06 2020-04-30 Vertex Pharmaceuticals Inc. Związek 2-amino-6-fluoro-n-[5-fluoro-pirydyn-3-ylo]pyrazolo [1,5-a]pirymidino-3-karboksamidu przydatny jako inhibitor kinazy atr, jego wytwarzanie, różne postacie stałe i ich radioznakowane pochodne
SG10201902206QA (en) 2014-06-05 2019-04-29 Vertex Pharma Radiolabelled derivatives of a 2-amino-6-fluoro-n-[5-fluoro-pyridin-3-yl]- pyrazolo[1,5-a]pyrimidin-3-carboxamide compound useful as atr kinase inhibitor, the preparation of said compound and different solid forms thereof
PT3157566T (pt) 2014-06-17 2019-07-11 Vertex Pharma Método para tratamento de cancro utilizando uma combinação de inibidores chk1 e atr
AU2016205361C1 (en) 2015-01-06 2021-04-08 Arena Pharmaceuticals, Inc. Methods of treating conditions related to the S1P1 receptor
MY192358A (en) 2015-05-20 2022-08-17 Idorsia Pharmaceuticals Ltd Crystalline form of the compound (s)-3-{4-[5-(2-cyclopentyl-6-methoxy-pyridin-4-yl)-[1,2,4]oxadiazol-3-yl]-2-ethyl-6-methyl-phenoxy}-propane-1,2-diol
CA3002551A1 (en) 2015-06-22 2016-12-29 Arena Pharmaceuticals, Inc. Crystalline l-arginine salt of (r)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclo-penta[b]indol-3-yl)acetic acid(com pound 1)for use in s1p1 receptor-associated disorders
RU2768621C1 (ru) 2015-09-30 2022-03-24 Вертекс Фармасьютикалз Инкорпорейтед Способ лечения рака с использованием комбинации повреждающих днк средств и ингибиторов atr
WO2018151834A1 (en) 2017-02-16 2018-08-23 Arena Pharmaceuticals, Inc. Compounds and methods for treatment of inflammatory bowel disease with extra-intestinal manifestations
CA3053418A1 (en) 2017-02-16 2018-08-23 Arena Pharmaceuticals, Inc. Compounds and methods for treatment of primary biliary cholangitis
CN108178759B (zh) * 2018-01-05 2020-06-09 上海瑞纷医药科技有限责任公司 一种α-肾上腺素受体拮抗剂的合成方法
CA3102136A1 (en) 2018-06-06 2019-12-12 Arena Pharmaceuticals, Inc. Methods of treating conditions related to the s1p1 receptor
CN119751336A (zh) 2018-09-06 2025-04-04 艾尼纳制药公司 可用于治疗自身免疫性病症和炎性病症的化合物
WO2025151705A1 (en) * 2024-01-10 2025-07-17 Vrise Therapeutics, Inc. Novel inhibitors of dna damage repair pathway

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3647809A (en) * 1968-04-26 1972-03-07 Chinoin Gyogyszer Es Vegyeszet Certain pyridyl-1 2 4-oxadiazole derivatives
PL353825A1 (en) * 1999-08-19 2003-12-01 Nps Pharmaceuticals, Inc.Nps Pharmaceuticals, Inc. Heteropolycyclic compounds and their use as metabotropic glutamate receptor antagonists
EP1379525B1 (en) * 2001-02-21 2007-10-10 Nps Pharmaceuticals, Inc. Heteropolycyclic compounds and their use as metabotropic glutamate receptor antagonists
ATE441654T1 (de) * 2002-01-18 2009-09-15 Merck & Co Inc Edg-rezeptoragonisten
CA2488117A1 (en) * 2002-06-17 2003-12-24 Merck & Co., Inc. 1-((5-aryl-1,2,4-oxadiazol-3-yl)benzyl)azetidine-3-carboxylates and 1-((5-aryl-1,2,4-oxadiazol-3-yl)benzyl)pyrrolidine-3-carboxylates as edg receptor agonists

Also Published As

Publication number Publication date
EP1625123A2 (en) 2006-02-15
EP1625123A4 (en) 2007-08-29
CN1788008A (zh) 2006-06-14
WO2004103279A2 (en) 2004-12-02
AU2004240586A1 (en) 2004-12-02
WO2004103279A3 (en) 2005-05-19
JP2006528980A (ja) 2006-12-28
US20060252741A1 (en) 2006-11-09

Similar Documents

Publication Publication Date Title
CA2524867A1 (en) 3-(2-amino-1-azacyclyl)-5-aryl-1,2,4-oxadiazoles as s1p receptor agonists
CA2509218C (en) 1-(amino)indanes and (1,2-dihydro-3-amino)-benzofurans, benzothiophenes and indoles as edg receptor agonists
US20070043014A1 (en) 3,5-Aryl, heteroaryl or cycloalkyl substituted-1,2,4-oxadiazoles as s1p receptor agonists
US7199142B2 (en) 1-((5-aryl-1,2,4-oxadiazol-3-yl) benzyl)azetidine-3-carboxylates and 1-((5-aryl-1,2,4-oxadiazol-3-yl)benzyl) pyrrolidine-3-carboxylates as edg receptor agonists
US7479504B2 (en) Edg receptor agonists
JP4709488B2 (ja) Edg受容体作動薬としてのN−(ベンジル)アミノアルキルカルボン酸化合物、ホスフィン酸化合物、ホスホン酸化合物およびテトラゾール類
AU2005299851B2 (en) 2-(aryl)azacyclylmethyl carboxylates, sulfonates, phosphonates, phosphinates and heterocycles as S1P receptor agonists
JP2005531506A (ja) Edg受容体作動薬としてのアミノアルキルホスホネートおよび関連化合物
WO2003074008A2 (en) Aminoalkylphosphonates and related compounds as edg receptor agonists
AU2003202994A1 (en) N-(benzyl)aminoalkylcarboxylates, phosphinates, phosphonates and tetrazoles as Edg receptor agonists

Legal Events

Date Code Title Description
FZDE Discontinued