CN103097365B - 作为鞘氨醇-1-磷酸(s1p)受体上的配体的5-(联苯-4-基)-3-苯基-1,2,4-噁二唑基衍生物 - Google Patents

作为鞘氨醇-1-磷酸(s1p)受体上的配体的5-(联苯-4-基)-3-苯基-1,2,4-噁二唑基衍生物 Download PDF

Info

Publication number
CN103097365B
CN103097365B CN201180033823.9A CN201180033823A CN103097365B CN 103097365 B CN103097365 B CN 103097365B CN 201180033823 A CN201180033823 A CN 201180033823A CN 103097365 B CN103097365 B CN 103097365B
Authority
CN
China
Prior art keywords
methyl
tert
formula
ethyl
amino
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.)
Expired - Fee Related
Application number
CN201180033823.9A
Other languages
English (en)
Chinese (zh)
Other versions
CN103097365A (zh
Inventor
A.博姆布伦
A.夸特罗帕尼
J.冈萨莱斯
J.多尔拜斯
C.奈特
C.巴克-格伦
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 Serono SA
Original Assignee
Merck Serono SA
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 Merck Serono SA filed Critical Merck Serono SA
Publication of CN103097365A publication Critical patent/CN103097365A/zh
Application granted granted Critical
Publication of CN103097365B publication Critical patent/CN103097365B/zh
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
    • C07D271/02—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
    • C07D271/06—1,2,4-Oxadiazoles; Hydrogenated 1,2,4-oxadiazoles
    • 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
    • A61K31/4245—Oxadiazoles
    • 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
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • 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
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
    • 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
    • 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
    • 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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Neurology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • Dermatology (AREA)
  • Gastroenterology & Hepatology (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)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201180033823.9A 2010-07-08 2011-07-06 作为鞘氨醇-1-磷酸(s1p)受体上的配体的5-(联苯-4-基)-3-苯基-1,2,4-噁二唑基衍生物 Expired - Fee Related CN103097365B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
EP10168833.1 2010-07-08
EP10168833 2010-07-08
US36274610P 2010-07-09 2010-07-09
US61/362746 2010-07-09
PCT/EP2011/061372 WO2012004287A1 (en) 2010-07-08 2011-07-06 5-(biphenyl-4-yl)-3-phenyl-1,2,4-oxadiazolyl derivatives as ligands on the sphingosine 1-phosphate (s1p) receptors

Publications (2)

Publication Number Publication Date
CN103097365A CN103097365A (zh) 2013-05-08
CN103097365B true CN103097365B (zh) 2016-02-24

Family

ID=42341535

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201180033823.9A Expired - Fee Related CN103097365B (zh) 2010-07-08 2011-07-06 作为鞘氨醇-1-磷酸(s1p)受体上的配体的5-(联苯-4-基)-3-苯基-1,2,4-噁二唑基衍生物

Country Status (15)

Country Link
US (1) US9029405B2 (https=)
EP (1) EP2590956B1 (https=)
JP (1) JP6014589B2 (https=)
KR (1) KR20140003379A (https=)
CN (1) CN103097365B (https=)
AR (1) AR082132A1 (https=)
AU (1) AU2011275854B2 (https=)
CA (1) CA2804473C (https=)
EA (1) EA201300092A1 (https=)
ES (1) ES2586145T3 (https=)
IL (1) IL224071B (https=)
MX (1) MX2012015021A (https=)
SG (1) SG186872A1 (https=)
TW (1) TW201206429A (https=)
WO (1) WO2012004287A1 (https=)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102250035A (zh) * 2011-06-10 2011-11-23 北京富卡生物技术有限公司 二芳基取代-1，3，4-噁二唑化合物的合成方法和其药物用途
CN107857760A (zh) * 2017-11-21 2018-03-30 南京天翔医药科技有限公司 鞘氨醇‑1‑磷酸受体调节剂及其应用
JP7679384B2 (ja) * 2019-12-23 2025-05-19 シトリクス・セラピューティクス・リミテッド 抗炎症特性を有するカルボン酸誘導体
KR20220158743A (ko) * 2020-03-27 2022-12-01 리셉토스 엘엘씨 스핑고신 1 포스페이트 수용체 조절제
US20240228448A1 (en) * 2021-03-31 2024-07-11 Washington University Compositions for binding sphingosine-1-phosphate receptor 1 (s1p1), imaging of s1p1, and processes for preparation thereof
KR102658761B1 (ko) * 2021-04-14 2024-04-19 주식회사 엘지화학 스핑고신-1-인산 수용체 효능제 합성을 위한 중간체의 제조방법
US12571867B2 (en) 2022-04-14 2026-03-10 United States Pharmacopeial Convention Nuclear magnetic resonance analysis systems and methods

Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1894225A (zh) * 2003-12-17 2007-01-10 默克公司 作为鞘氨醇1－磷酸(内皮分化基因)受体激动剂的(3,4－二取代)丙酸酯
WO2008037476A1 (en) * 2006-09-29 2008-04-03 Novartis Ag Oxadiazole derivatives with anti-inflammatory and immunosuppressive properties
CN101184739A (zh) * 2005-06-08 2008-05-21 诺瓦提斯公司 多环二唑类和异唑类化合物及其作为s1p受体的配体的用途
US20080200535A1 (en) * 2006-08-25 2008-08-21 Asahi Kasei Pharma Corporation Amine Compounds
CN101374821A (zh) * 2006-01-27 2009-02-25 诺瓦提斯公司 作为s1p1受体激动剂、免疫抑制剂和抗炎药的3,5－二(芳基或杂芳基)异唑和1,2,4－二唑类
WO2009043889A2 (en) * 2007-10-04 2009-04-09 Merck Serono S.A. Oxadiazole derivatives
WO2010112461A1 (en) * 2009-04-03 2010-10-07 Merck Serono S.A. Oxadiazole derivatives

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0711792B1 (de) 1994-11-05 1999-03-10 BASF Aktiengesellschaft Melaminharze
US20060223866A1 (en) * 2004-08-13 2006-10-05 Praecis Pharmaceuticals, Inc. Methods and compositions for modulating sphingosine-1-phosphate (S1P) receptor activity
BRPI0612028A2 (pt) * 2005-06-08 2010-10-13 Novartis Ag oxadiazóis ou isodiazóis policìclicos e uso dos mesmos como ligantes de receptor s1p
TWI404706B (zh) * 2006-01-11 2013-08-11 Actelion Pharmaceuticals Ltd 新穎噻吩衍生物
TW201000099A (en) * 2008-06-20 2010-01-01 Amgen Inc S1P1 receptor agonists and use thereof

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1894225A (zh) * 2003-12-17 2007-01-10 默克公司 作为鞘氨醇1－磷酸(内皮分化基因)受体激动剂的(3,4－二取代)丙酸酯
CN101184739A (zh) * 2005-06-08 2008-05-21 诺瓦提斯公司 多环二唑类和异唑类化合物及其作为s1p受体的配体的用途
CN101374821A (zh) * 2006-01-27 2009-02-25 诺瓦提斯公司 作为s1p1受体激动剂、免疫抑制剂和抗炎药的3,5－二(芳基或杂芳基)异唑和1,2,4－二唑类
US20080200535A1 (en) * 2006-08-25 2008-08-21 Asahi Kasei Pharma Corporation Amine Compounds
WO2008037476A1 (en) * 2006-09-29 2008-04-03 Novartis Ag Oxadiazole derivatives with anti-inflammatory and immunosuppressive properties
WO2009043889A2 (en) * 2007-10-04 2009-04-09 Merck Serono S.A. Oxadiazole derivatives
WO2010112461A1 (en) * 2009-04-03 2010-10-07 Merck Serono S.A. Oxadiazole derivatives

Also Published As

Publication number Publication date
JP6014589B2 (ja) 2016-10-25
CN103097365A (zh) 2013-05-08
AU2011275854B2 (en) 2015-08-27
EA201300092A1 (ru) 2013-06-28
IL224071B (en) 2018-06-28
ES2586145T3 (es) 2016-10-11
AR082132A1 (es) 2012-11-14
AU2011275854A1 (en) 2013-02-21
WO2012004287A1 (en) 2012-01-12
CA2804473C (en) 2019-04-02
JP2013530202A (ja) 2013-07-25
TW201206429A (en) 2012-02-16
US9029405B2 (en) 2015-05-12
CA2804473A1 (en) 2012-01-12
KR20140003379A (ko) 2014-01-09
SG186872A1 (en) 2013-02-28
US20130116289A1 (en) 2013-05-09
MX2012015021A (es) 2013-04-03
EP2590956B1 (en) 2016-05-04
EP2590956A1 (en) 2013-05-15

Similar Documents

Publication Publication Date Title
ES2639028T3 (es) Derivados de oxadiazol
CN103097365B (zh) 作为鞘氨醇-1-磷酸(s1p)受体上的配体的5-(联苯-4-基)-3-苯基-1,2,4-噁二唑基衍生物
CA2763683C (en) Pyrazole oxadiazole derivatives as s1p1 agonists
US8741923B2 (en) Oxadiazole fused heterocyclic derivatives useful for the treatment of multiple sclerosis
CA2752804C (en) Oxazole pyridine derivatives useful as s1p1 receptor agonists
HK1181035A (en) 5-(biphenyl-4-yl)-3-phenyl-1,2,4-oxadiazolyl derivatives as ligands on the sphingosine 1-phosphate (s1p) receptors
HK1174915A (en) Oxadiazole derivatives
HK1161244A (en) Oxadiazole fused heterocyclic derivatives useful for the treatment of multiple sclerosis

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 1181035

Country of ref document: HK

C14 Grant of patent or utility model
GR01 Patent grant
REG Reference to a national code

Ref country code: HK

Ref legal event code: WD

Ref document number: 1181035

Country of ref document: HK

CF01 Termination of patent right due to non-payment of annual fee

Granted publication date: 20160224

Termination date: 20210706

CF01 Termination of patent right due to non-payment of annual fee