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)
Other versions
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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Filing date
Publication date
Priority claimed from GB0329500A external-priority patent/GB0329500D0/en
Priority claimed from GB0329505A external-priority patent/GB0329505D0/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)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Immunology (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (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
GB0329505.2 2003-12-19
GB0329500A GB0329500D0 (en) 2003-12-19 2003-12-19 Organic compounds
GB0329500.3 2003-12-19
GB0329505A GB0329505D0 (en) 2003-12-19 2003-12-19 Organic compounds
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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EP1546110A4 (en) 2002-07-30 2008-03-26 Univ Virginia COMPOUNDS WITH EFFECT ON SIGNAL TRANSMISSION BY SPHINGOSINE-1-PHOSPHATE
GB0313612D0 (en) * 2003-06-12 2003-07-16 Novartis Ag Organic compounds
MXPA06002349A (es) 2003-08-28 2006-05-22 Novartis Ag Derivados de aminopropanol.
US7638637B2 (en) 2003-11-03 2009-12-29 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
AU2005264431B2 (en) * 2004-07-16 2010-08-19 Kyorin Pharmaceutical Co., Ltd. Method of effectively using medicine and method concerning prevention of side effect
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)
PT2511262T (pt) 2004-10-12 2017-03-30 Kyorin Seiyaku Kk Processo para a produção de cloridrato de 2-amino-2-[2-[4-(3- benziloxi-feniltio)-2-clorofenil[etil]-1,3-propanodiol
JP2008530135A (ja) 2005-02-14 2008-08-07 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 アミノ基およびフェニル基で置換されたシクロアルカンならびに５員の複素環を含むスフィンゴシン＝１−リン酸アゴニスト
GB0513431D0 (en) 2005-06-30 2005-08-10 Kherion Technology Ltd Prophylactic compositions and uses
BRPI0617077A2 (pt) * 2005-10-07 2015-01-06 Kyorin Seiyaku Kk Agente terapêutico para tratamento de doenças do fígado contendo 2-amina-1, 3-propanediol derivativo como ingrediente ativo, e método para tratamento de doenças do fígado
BRPI0619894B8 (pt) 2005-12-15 2021-05-25 Mitsubishi Tanabe Pharma Corp composto de amina e composição farmacêutica
EP1986623A2 (en) 2006-01-27 2008-11-05 University Of Virginia Patent Foundation Method for treatment of neuropathic pain
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
JP2009526073A (ja) 2006-02-09 2009-07-16 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 二環式スフィンゴシン−１−リン酸受容体アナログ
WO2007112322A2 (en) 2006-03-28 2007-10-04 Allergan, Inc. Indole compounds having sphingosine-1-phosphate (s1p) receptor agonist and/or antagonist biological activity
CA2659599C (en) 2006-08-08 2014-06-17 Kyorin Pharmaceutical Co., Ltd. Amino alcohol derivative and immunosuppressive agent having same as an active ingredient
NZ574011A (en) * 2006-08-08 2011-10-28 Kyorin Seiyaku Kk Aminophosphoric acid ester derivative and s1p receptor modulator containing the same as active ingredient
NZ576893A (en) 2006-11-21 2012-01-12 Univ Virginia Patent Found Tetralin analogs having sphingosine 1-phosphate agonist activity
WO2008064320A2 (en) 2006-11-21 2008-05-29 University Of Virginia Patent Foundation Hydrindane analogs having sphingosine 1-phosphate receptor agonist activity
EP2097371A2 (en) 2006-11-21 2009-09-09 University Of Virginia Patent Foundation Benzocycloheptyl analogs having sphingosine 1-phosphate receptor 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
KR101161498B1 (ko) * 2007-06-14 2012-06-29 미쓰비시 타나베 파마 코퍼레이션 아민 화합물 및 그 의약 용도
US7888336B2 (en) 2007-09-24 2011-02-15 Allergan, Inc. Indole compounds bearing aryl or heteroaryl groups having sphingosine 1-phosphate (S1P) receptor biological activity
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
WO2009137342A1 (en) 2008-05-08 2009-11-12 Allergan, Inc. Therapeutically useful substituted 1, 7-diphenyl-l, 2, 3, 5, 6, 7-hexahydropyrido [ 3, 2, 1-i j ] 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
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
CN105816453B (zh) 2008-08-27 2021-03-05 艾尼纳制药公司 用于治疗自身免疫性病症和炎性病症的作为s1p1受体激动剂的经取代的三环酸衍生物
US9073888B2 (en) * 2009-10-23 2015-07-07 Allergan, Inc. Coumarin compounds as receptor modulators with therapeutic utility
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CA2789480A1 (en) 2010-03-03 2011-09-09 Arena Pharmaceuticals, Inc. Processes for the preparation of s1p1 receptor modulators and crystalline forms thereof
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
US11007175B2 (en) 2015-01-06 2021-05-18 Arena Pharmaceuticals, Inc. Methods of treating conditions related to the S1P1 receptor
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JP2020507610A (ja) 2017-02-16 2020-03-12 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 腸管外症状を伴う炎症性腸疾患の治療のための化合物および方法
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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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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
AU2004234066A1 (en) 2004-11-11
JP4603531B2 (ja) 2010-12-22
MXPA05011596A (es) 2006-01-23
JP2006524660A (ja) 2006-11-02
EP1622860B1 (en) 2012-02-29
EP1622860A1 (en) 2006-02-08
CA2523582A1 (en) 2004-11-11
CN1777575A (zh) 2006-05-24
US7625950B2 (en) 2009-12-01
ES2383298T3 (es) 2012-06-20
AU2004234066B2 (en) 2008-02-21
BRPI0410025A (pt) 2006-04-25
ATE547395T1 (de) 2012-03-15
US20060211658A1 (en) 2006-09-21
WO2004096752A1 (en) 2004-11-11

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Granted publication date: 20100512

Termination date: 20130429