CN1777575B - 作为1-磷酸-鞘氨醇受体调节剂的氨基-丙醇衍生物 - Google Patents

作为1-磷酸-鞘氨醇受体调节剂的氨基-丙醇衍生物 Download PDF

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Publication number
CN1777575B
CN1777575B CN2004800110595A CN200480011059A CN1777575B CN 1777575 B CN1777575 B CN 1777575B CN 2004800110595 A CN2004800110595 A CN 2004800110595A CN 200480011059 A CN200480011059 A CN 200480011059A CN 1777575 B CN1777575 B CN 1777575B
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CN
China
Prior art keywords
alkyl
phenyl
compound
formula
cycloalkyl
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
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CN2004800110595A
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English (en)
Chinese (zh)
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CN1777575A (zh
Inventor
K·欣特尔丁
C·斯庞克
F·泽克里
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Novartis AG
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Novartis AG
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Publication date
Priority claimed from GB0329505A external-priority patent/GB0329505D0/en
Priority claimed from GB0329500A external-priority patent/GB0329500D0/en
Application filed by Novartis AG filed Critical Novartis AG
Publication of CN1777575A publication Critical patent/CN1777575A/zh
Application granted granted Critical
Publication of CN1777575B publication Critical patent/CN1777575B/zh
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D317/00—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
    • C07D317/08—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3
    • C07D317/44—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D317/46—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C07D317/48—Methylenedioxybenzenes or hydrogenated methylenedioxybenzenes, unsubstituted on the hetero ring
    • C07D317/62—Methylenedioxybenzenes or hydrogenated methylenedioxybenzenes, unsubstituted on the hetero ring 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 atoms of the carbocyclic ring
    • C07D317/64—Oxygen atoms
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C217/00—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton
    • C07C217/54—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
    • C07C217/64—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains further substituted by singly-bound oxygen atoms
    • C07C217/66—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains further substituted by singly-bound oxygen atoms with singly-bound oxygen atoms and six-membered aromatic rings bound to the same carbon atom of the carbon chain
    • C07C217/72—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains further substituted by singly-bound oxygen atoms with singly-bound oxygen atoms and six-membered aromatic rings bound to the same carbon atom of the carbon chain linked by carbon chains having at least three carbon atoms between the amino groups and the six-membered aromatic ring or the condensed ring system containing that ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/06—Phosphorus compounds without P—C bonds
    • C07F9/08—Esters of oxyacids of phosphorus
    • C07F9/09—Esters of phosphoric acids
    • C07F9/094—Esters of phosphoric acids with arylalkanols
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6564—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms
    • C07F9/6571—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and oxygen atoms as the only ring hetero atoms
    • C07F9/6574—Esters of oxyacids of phosphorus
    • C07F9/65744—Esters of oxyacids of phosphorus condensed with carbocyclic or heterocyclic rings or ring systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Immunology (AREA)
  • Molecular Biology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Biochemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Heterocyclic Compounds That Contain Two Or More Ring Oxygen Atoms (AREA)
CN2004800110595A 2003-04-30 2004-04-29 作为1-磷酸-鞘氨醇受体调节剂的氨基-丙醇衍生物 Expired - Fee Related CN1777575B (zh)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
GB0309944.7 2003-04-30
GB0309944 2003-04-30
GB0329505A GB0329505D0 (en) 2003-12-19 2003-12-19 Organic compounds
GB0329505.2 2003-12-19
GB0329500A GB0329500D0 (en) 2003-12-19 2003-12-19 Organic compounds
GB0329500.3 2003-12-19
PCT/EP2004/004569 WO2004096752A1 (en) 2003-04-30 2004-04-29 Amino-propanol derivatives as sphingosine-1-phosphate receptor modulator

Publications (2)

Publication Number Publication Date
CN1777575A CN1777575A (zh) 2006-05-24
CN1777575B true CN1777575B (zh) 2010-05-12

Family

ID=33424535

Family Applications (1)

Application Number Title Priority Date Filing Date
CN2004800110595A Expired - Fee Related CN1777575B (zh) 2003-04-30 2004-04-29 作为1-磷酸-鞘氨醇受体调节剂的氨基-丙醇衍生物

Country Status (11)

Country Link
US (1) US7625950B2 (enExample)
EP (1) EP1622860B1 (enExample)
JP (1) JP4603531B2 (enExample)
CN (1) CN1777575B (enExample)
AT (1) ATE547395T1 (enExample)
AU (1) AU2004234066B2 (enExample)
BR (1) BRPI0410025A (enExample)
CA (1) CA2523582A1 (enExample)
ES (1) ES2383298T3 (enExample)
MX (1) MXPA05011596A (enExample)
WO (1) WO2004096752A1 (enExample)

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AU2003259296A1 (en) 2002-07-30 2004-02-16 University Of Virginia Patent Foundation Compounds active in spinigosine 1-phosphate signaling
GB0313612D0 (en) * 2003-06-12 2003-07-16 Novartis Ag Organic compounds
EP1660449B1 (en) * 2003-08-28 2009-11-18 Novartis AG Aminopropanol derivatives
WO2005041899A2 (en) 2003-11-03 2005-05-12 University Of Virginia Patent Foundation Orally available sphingosine 1-phosphate receptor agonists and antagonists
GB0329498D0 (en) * 2003-12-19 2004-01-28 Novartis Ag Organic compounds
WO2006001463A1 (ja) * 2004-06-23 2006-01-05 Ono Pharmaceutical Co., Ltd. Ｓ１ｐ受容体結合能を有する化合物およびその用途
CN101905023B (zh) * 2004-07-16 2012-07-11 杏林制药株式会社 有效的医药使用方法及与副作用发生的防御相关的方法
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)
PL1806338T3 (pl) 2004-10-12 2016-07-29 Kyorin Seiyaku Kk Sposób wytwarzania chlorowodorku 2-amino-2-[2-[4-(3-benzyloksyfenylotio)-2-chlorofenyio]etylo]-1,3-propanodioiu i jego hydratów oraz produkty pośrednie w ich wytwarzaniu
CA2596990A1 (en) 2005-02-14 2006-08-24 University Of Virginia Patent Foundation Sphingosine 1-phosphate agonists comprising cycloalkanes and 5 -membered heterocycles substituted by amino and phenyl groups
GB0513431D0 (en) 2005-06-30 2005-08-10 Kherion Technology Ltd Prophylactic compositions and uses
SI1932522T1 (sl) * 2005-10-07 2012-08-31 Kyorin Seiyaku Kk Terapevtsko sredstvo za jetrno bolezen, ki vsebuje 2-amino-1,3- propandiolni derivat kot aktivno sestavino
RU2433117C2 (ru) 2005-12-15 2011-11-10 Мицубиси Танабе Фарма Корпорейшн Аминное соединение и его применение в медицинских целях
KR20080086546A (ko) 2006-01-27 2008-09-25 유니버시티 오브 버지니아 페이턴트 파운데이션 신경병증성 통증의 치료 방법
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
WO2007092638A1 (en) 2006-02-09 2007-08-16 University Of Virginia Patent Foundation Bicyclic sphingosine 1-phosphate analogs
US8097644B2 (en) 2006-03-28 2012-01-17 Allergan, Inc. Indole compounds having sphingosine-1-phosphate (S1P) receptor antagonist
RU2430925C2 (ru) 2006-08-08 2011-10-10 Киорин Фармасьютикал Ко., Лтд. Производное аминофосфата и модулятор рецептора s1p, содержащий его в качестве активного ингредиента
CA2659599C (en) 2006-08-08 2014-06-17 Kyorin Pharmaceutical Co., Ltd. Amino alcohol derivative and immunosuppressive agent having same as an active ingredient
JP2010510250A (ja) 2006-11-21 2010-04-02 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 スフィンゴシン＝１−燐酸受容体アゴニスト活性を有するヒドリンダンアナログ
JP2010510251A (ja) 2006-11-21 2010-04-02 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 スフィンゴシン＝１−燐酸受容体活性を有するベンゾシクロヘプチルアナログ
AU2007323618A1 (en) 2006-11-21 2008-05-29 University Of Virginia Patent Foundation Tetralin analogs having sphingosine 1-phosphate agonist activity
US8524917B2 (en) 2007-01-11 2013-09-03 Allergan, Inc. 6-substituted indole-3-carboxylic acid amide compounds having sphingosine-1-phosphate (S1P) receptor antagonist biological activity
BRPI0813683A2 (pt) * 2007-06-14 2019-09-24 Mitsubishi Tanabe Pharma Corp composto amina e uso farmacêutico do mesmo
BRPI0817397A2 (pt) 2007-09-24 2015-04-07 Allergan Inc Compostos indol contendo grupos arila ou heteroarila com atividade biológica do receptor de esfingosina-1-fosfato (sip)
JP5452237B2 (ja) 2008-02-07 2014-03-26 杏林製薬株式会社 アミノアルコール誘導体を有効成分とする炎症性腸疾患の治療剤又は予防剤
CA2723775A1 (en) 2008-05-08 2009-11-12 Allergan, Inc. Therapeutically useful substituted 1,7-diphenyl-1,2,3,5,6,7-hexahydropyrido[3,2,1-ij]quinoline compounds
US8143291B2 (en) 2008-05-09 2012-03-27 Allergan, Inc. Indole compounds bearing aryl or heteroaryl groups having sphingosine-1-phosphate (S1P) receptor biological activity
CN104311472B9 (zh) 2008-07-23 2020-03-17 艾尼纳制药公司 经取代的1,2,3,4-四氢环戊并[b]吲哚-3-基乙酸衍生物
PL2342205T4 (pl) 2008-08-27 2016-12-30 Podstawione tricykliczne pochodne kwasowe jako antagoniści receptora S1P1 użyteczni w leczeniu zaburzeń autoimmunologicznych i zapalnych
KR20120075481A (ko) * 2009-10-23 2012-07-06 알러간, 인코포레이티드 치료적 유용성을 갖는 수용체 조절제로서 쿠마린 화합물
CA2780859A1 (en) * 2009-12-10 2011-06-16 Novartis Ag Fty720 halogenated derivatives
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CN105503882B (zh) 2010-03-03 2019-07-05 艾尼纳制药公司 制备s1p1受体调节剂及其晶体形式的方法
CN102260178A (zh) * 2010-05-25 2011-11-30 中国医学科学院药物研究所 羟基丙二醇类衍生物、其制备方法和其药物组合物与用途
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JP6838744B2 (ja) 2015-06-22 2021-03-03 アリーナ ファーマシューティカルズ， インコーポレイテッド Ｓ１Ｐ１レセプター関連障害における使用のための（Ｒ）−２−（７−（４−シクロペンチル−３−（トリフルオロメチル）ベンジルオキシ）−１，２，３，４−テトラヒドロシクロペンタ［ｂ］インドール−３−イル）酢酸（化合物１）の結晶性Ｌ−アルギニン塩
CN110520124A (zh) 2017-02-16 2019-11-29 艾尼纳制药公司 用于治疗原发性胆汁性胆管炎的化合物和方法
KR20190113955A (ko) 2017-02-16 2019-10-08 아레나 파마슈티칼스, 인크. 장-외 증상을 갖는 염증성 장질환의 치료를 위한 화합물 및 방법
JP7397011B2 (ja) 2018-06-06 2023-12-12 アリーナ ファーマシューティカルズ， インコーポレイテッド Ｓ１ｐ１受容体に関連する状態を治療する方法
EP3847158B1 (en) 2018-09-06 2026-06-24 Arena Pharmaceuticals, Inc. Compounds useful in the treatment of autoimmune and inflammatory disorders

Citations (2)

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Publication number Priority date Publication date Assignee Title
EP0778263A1 (en) * 1994-08-22 1997-06-11 Yoshitomi Pharmaceutical Industries, Ltd. Benzene compound and medicinal use thereof
EP1002792A1 (en) * 1997-04-04 2000-05-24 Yoshitomi Pharmaceutical Industries, Ltd. 2-aminopropane-1,3-diol compounds, medicinal use thereof, and intermediates in synthesizing the same

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KR100913269B1 (ko) * 2001-09-27 2009-08-21 교린 세이야꾸 가부시키 가이샤 디아릴 황화물 유도체, 그의 염 및 이를 이용한 면역억제제
CN100516024C (zh) 2002-09-13 2009-07-22 诺瓦提斯公司 氨基-丙醇衍生物

Patent Citations (2)

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Publication number Priority date Publication date Assignee Title
EP0778263A1 (en) * 1994-08-22 1997-06-11 Yoshitomi Pharmaceutical Industries, Ltd. Benzene compound and medicinal use thereof
EP1002792A1 (en) * 1997-04-04 2000-05-24 Yoshitomi Pharmaceutical Industries, Ltd. 2-aminopropane-1,3-diol compounds, medicinal use thereof, and intermediates in synthesizing the same

Also Published As

Publication number Publication date
AU2004234066B2 (en) 2008-02-21
EP1622860B1 (en) 2012-02-29
EP1622860A1 (en) 2006-02-08
AU2004234066A1 (en) 2004-11-11
WO2004096752A1 (en) 2004-11-11
JP2006524660A (ja) 2006-11-02
ES2383298T3 (es) 2012-06-20
US20060211658A1 (en) 2006-09-21
US7625950B2 (en) 2009-12-01
MXPA05011596A (es) 2006-01-23
JP4603531B2 (ja) 2010-12-22
BRPI0410025A (pt) 2006-04-25
ATE547395T1 (de) 2012-03-15
CN1777575A (zh) 2006-05-24
CA2523582A1 (en) 2004-11-11

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