WO2009017219A1 - Ｓ１ｐ1結合阻害物質 - Google Patents

Ｓ１ｐ1結合阻害物質 Download PDF

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Publication number
WO2009017219A1
WO2009017219A1 PCT/JP2008/063851 JP2008063851W WO2009017219A1 WO 2009017219 A1 WO2009017219 A1 WO 2009017219A1 JP 2008063851 W JP2008063851 W JP 2008063851W WO 2009017219 A1 WO2009017219 A1 WO 2009017219A1
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Prior art keywords
formula
nitrogen atom
group
group represented
crb
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PCT/JP2008/063851
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English (en)
French (fr)
Inventor
Naoya Ono
Fumiyasu Shiozawa
Tetsuya Yabuuchi
Hironori Katakai
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Taisho Pharmaceutical Co., Ltd.
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Publication date
Priority to PL08792064T priority Critical patent/PL2177512T3/pl
Priority to AT08792064T priority patent/ATE554070T1/de
Priority to CN2008801013035A priority patent/CN101790517B/zh
Priority to JP2009525458A priority patent/JP5311057B2/ja
Priority to ES08792064T priority patent/ES2382697T3/es
Priority to US12/671,401 priority patent/US8048898B2/en
Priority to RS20120266A priority patent/RS52368B/en
Priority to SI200830618T priority patent/SI2177512T1/sl
Application filed by Taisho Pharmaceutical Co., Ltd. filed Critical Taisho Pharmaceutical Co., Ltd.
Priority to DK08792064.1T priority patent/DK2177512T3/da
Priority to EP08792064A priority patent/EP2177512B1/en
Priority to RU2010107211/04A priority patent/RU2468009C2/ru
Publication of WO2009017219A1 publication Critical patent/WO2009017219A1/ja
Priority to HK10110155.8A priority patent/HK1143591A1/xx
Priority to HRP20120363AT priority patent/HRP20120363T1/hr

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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 ring carbon atoms
    • C07D213/62—Oxygen or sulfur atoms
    • C07D213/63—One oxygen atom
    • C07D213/64—One oxygen atom attached in position 2 or 6
    • 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
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    • A61P11/00—Drugs for disorders of the respiratory system
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • 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
    • A61P35/00—Antineoplastic agents
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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 ring carbon atoms
    • C07D213/62—Oxygen or sulfur atoms
    • C07D213/63—One oxygen atom
    • C07D213/68—One oxygen atom attached in position 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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 ring carbon atoms
    • C07D213/62—Oxygen or sulfur atoms
    • C07D213/70—Sulfur atoms
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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 ring carbon atoms
    • C07D213/62—Oxygen or sulfur atoms
    • C07D213/70—Sulfur atoms
    • C07D213/71—Sulfur atoms to which a second hetero atom is attached
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/34—One oxygen atom
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D—HETEROCYCLIC COMPOUNDS
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    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

Abstract

式（Ｉ） （式中、Ｙ1は窒素原子、またはＣＲAで表される基を示し、Ｙ2は窒素原子、またはＣＲBで表される基を示し、Ｙ3は窒素原子、またはＣＲCで表される基を示し、ＲA、ＲB、及びＲCはそれぞれ同一または異なって水素原子等を示し（ただしＹ1がＣＲA、Ｙ2がＣＲB、Ｙ3がＣＲCである場合を除く）、Xは酸素原子等を示し、Ｒ1は炭素原子数１～６個のアルキル基等を示し、Ｒ2は炭素原子数１～６個のアルキル基等を示し、Ｒ3は、置換されても良いフェニル基等を示し、Ｒ4は水素原子等を示し、Ｒ5は置換されても良いフェニル基等を示す。）で表される化合物またはその医薬上許容される塩は、Ｓ１Ｐとその受容体であるＥｄｇ－１（Ｓ１Ｐ1）との結合阻害作用を有し、自己免疫疾患、関節リウマチ、喘息、アトピー性皮膚炎、臓器移植後の拒絶反応、癌、網膜症、乾癬、変形性関節症、または加齢性黄斑変性症等の治療薬として有用である。
PCT/JP2008/063851 2007-08-01 2008-08-01 Ｓ１ｐ1結合阻害物質 WO2009017219A1 (ja)

Priority Applications (13)

Application Number Priority Date Filing Date Title
RS20120266A RS52368B (en) 2007-08-01 2008-08-01 S1P1 BINDING INHIBITORS
CN2008801013035A CN101790517B (zh) 2007-08-01 2008-08-01 抑制s1p1结合的物质
JP2009525458A JP5311057B2 (ja) 2007-08-01 2008-08-01 Ｓ１ｐ１結合阻害物質
ES08792064T ES2382697T3 (es) 2007-08-01 2008-08-01 Inhibidor de la unión de S1P1
US12/671,401 US8048898B2 (en) 2007-08-01 2008-08-01 Inhibitor of binding of S1P1
PL08792064T PL2177512T3 (pl) 2007-08-01 2008-08-01 Inhibitor wiązania S1P1
SI200830618T SI2177512T1 (sl) 2007-08-01 2008-08-01 Inhibitor vezave S1P1
AT08792064T ATE554070T1 (de) 2007-08-01 2008-08-01 Hemmer der s1p1-bindung
DK08792064.1T DK2177512T3 (da) 2007-08-01 2008-08-01 S1P1-bindingshæmmer
EP08792064A EP2177512B1 (en) 2007-08-01 2008-08-01 Inhibitor of binding of s1p1
RU2010107211/04A RU2468009C2 (ru) 2007-08-01 2008-08-01 Ингибитор связывания s1p1
HK10110155.8A HK1143591A1 (en) 2007-08-01 2010-10-28 Inhibitor of binding of s1p1
HRP20120363AT HRP20120363T1 (hr) 2007-08-01 2012-04-25 Inhibitor vezivanja s1p1

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2007201274 2007-08-01
JP2007-201274 2007-08-01

Publications (1)

Publication Number Publication Date
WO2009017219A1 true WO2009017219A1 (ja) 2009-02-05

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Application Number Title Priority Date Filing Date
PCT/JP2008/063851 WO2009017219A1 (ja) 2007-08-01 2008-08-01 Ｓ１ｐ1結合阻害物質

Country Status (16)

Country Link
US (1) US8048898B2 (ja)
EP (1) EP2177512B1 (ja)
JP (1) JP5311057B2 (ja)
CN (1) CN101790517B (ja)
AT (1) ATE554070T1 (ja)
CY (1) CY1113057T1 (ja)
DK (1) DK2177512T3 (ja)
ES (1) ES2382697T3 (ja)
HK (1) HK1143591A1 (ja)
HR (1) HRP20120363T1 (ja)
PL (1) PL2177512T3 (ja)
PT (1) PT2177512E (ja)
RS (1) RS52368B (ja)
RU (1) RU2468009C2 (ja)
SI (1) SI2177512T1 (ja)
WO (1) WO2009017219A1 (ja)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013064538A1 (en) * 2011-11-01 2013-05-10 Astex Therapeutics Limited Substituted benzylamine compounds, their use in medicine, and in particular the treatment of hepatitis c virus (hcv) infection
WO2019151470A1 (ja) 2018-02-02 2019-08-08 国立大学法人 京都大学 眼内血管新生及び／又は眼内血管透過性亢進を伴う眼科疾患の予防又は治療のための医薬

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