WO2010013805A1 - アミノプロピリデン誘導体 - Google Patents

アミノプロピリデン誘導体 Download PDF

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Publication number
WO2010013805A1
WO2010013805A1 PCT/JP2009/063645 JP2009063645W WO2010013805A1 WO 2010013805 A1 WO2010013805 A1 WO 2010013805A1 JP 2009063645 W JP2009063645 W JP 2009063645W WO 2010013805 A1 WO2010013805 A1 WO 2010013805A1
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WO
WIPO (PCT)
Prior art keywords
substituted
hydrogen
same
carbon
formula
Prior art date
Application number
PCT/JP2009/063645
Other languages
English (en)
French (fr)
Inventor
邦彦 東浦
尚志 荻野
泰三 伊藤
宏二 國増
Original Assignee
日本臓器製薬株式会社
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
Priority to PL09803043T priority Critical patent/PL2319840T3/pl
Priority to RU2011107744/04A priority patent/RU2483063C2/ru
Priority to CA2732282A priority patent/CA2732282C/en
Priority to KR1020117000685A priority patent/KR101375680B1/ko
Priority to US13/055,780 priority patent/US8653285B2/en
Priority to BRPI0917550A priority patent/BRPI0917550A2/pt
Priority to JP2010522760A priority patent/JP5379139B2/ja
Priority to ES09803043.0T priority patent/ES2561227T3/es
Application filed by 日本臓器製薬株式会社 filed Critical 日本臓器製薬株式会社
Priority to DK09803043.0T priority patent/DK2319840T3/en
Priority to CN200980130369.1A priority patent/CN102112462B/zh
Priority to AU2009277496A priority patent/AU2009277496B2/en
Priority to EP09803043.0A priority patent/EP2319840B1/en
Publication of WO2010013805A1 publication Critical patent/WO2010013805A1/ja
Priority to HK11113986.6A priority patent/HK1159612A1/xx

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/38Heterocyclic compounds having sulfur as a ring hetero atom
    • A61K31/381Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/4025Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/02Nasal agents, e.g. decongestants
    • 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
    • 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
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D333/00Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/50Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D333/78Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems condensed with rings other than six-membered or with ring systems containing such rings

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Otolaryngology (AREA)
  • Dermatology (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

本発明は式(I)で表される、優れたヒスタミン受容体拮抗作用を有する新規なアミノプロピリデン誘導体であり、医薬組成物、特に眠気等の中枢性副作用が少ない抗ヒスタミン薬等の有効成分として有用な化合物を提供する。〔式中、R1 及びR2 は同一若しくは異なって水素又は置換カルボニル、置換カルボニルアルキル、アクリル酸を表し(但し、両方が水素である場合を除く)、R3 及びR4 は同一若しくは異なって水素、フェニルで置換されていてもよいアルキル等を表し、A は無置換であるか又はオキソを表し、B は炭素又は酸素を表し、X 及びY はいずれか一方が炭素で他方が硫黄を表し、破線部分は単結合又は二重結合を表し、波線はシス体及び/又はトランス体を表す。〕
PCT/JP2009/063645 2008-08-01 2009-07-31 アミノプロピリデン誘導体 WO2010013805A1 (ja)

Priority Applications (13)

Application Number Priority Date Filing Date Title
JP2010522760A JP5379139B2 (ja) 2008-08-01 2009-07-31 アミノプロピリデン誘導体
CA2732282A CA2732282C (en) 2008-08-01 2009-07-31 Aminopropylidene derivative
KR1020117000685A KR101375680B1 (ko) 2008-08-01 2009-07-31 아미노프로필리덴 유도체
US13/055,780 US8653285B2 (en) 2008-08-01 2009-07-31 Aminopropylidene derivative
BRPI0917550A BRPI0917550A2 (pt) 2008-08-01 2009-07-31 derivado de aminopropilideno e composição farmacêutica compreendendo o referido derivado
PL09803043T PL2319840T3 (pl) 2008-08-01 2009-07-31 Pochodna aminopropylidenu
ES09803043.0T ES2561227T3 (es) 2008-08-01 2009-07-31 Derivado de aminopropilideno
RU2011107744/04A RU2483063C2 (ru) 2008-08-01 2009-07-31 Аминопропилиденовое производное
DK09803043.0T DK2319840T3 (en) 2008-08-01 2009-07-31 Aminopropylidene DERIVATIVE
CN200980130369.1A CN102112462B (zh) 2008-08-01 2009-07-31 氨基亚丙基衍生物
AU2009277496A AU2009277496B2 (en) 2008-08-01 2009-07-31 Aminopropylidene derivative
EP09803043.0A EP2319840B1 (en) 2008-08-01 2009-07-31 Aminopropylidene derivative
HK11113986.6A HK1159612A1 (en) 2008-08-01 2011-12-28 Aminopropylidene derivative

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
JP2008-199648 2008-08-01
JP2008199648 2008-08-01
JP2009-127385 2009-05-27
JP2009127385 2009-05-27

Publications (1)

Publication Number Publication Date
WO2010013805A1 true WO2010013805A1 (ja) 2010-02-04

Family

ID=41610499

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/JP2009/063645 WO2010013805A1 (ja) 2008-08-01 2009-07-31 アミノプロピリデン誘導体

Country Status (16)

Country Link
US (1) US8653285B2 (ja)
EP (1) EP2319840B1 (ja)
JP (2) JP5379139B2 (ja)
KR (1) KR101375680B1 (ja)
CN (2) CN104693215B (ja)
AU (1) AU2009277496B2 (ja)
BR (1) BRPI0917550A2 (ja)
CA (1) CA2732282C (ja)
DK (1) DK2319840T3 (ja)
ES (1) ES2561227T3 (ja)
HK (2) HK1159612A1 (ja)
PL (1) PL2319840T3 (ja)
PT (1) PT2319840E (ja)
RU (1) RU2483063C2 (ja)
TW (1) TWI457341B (ja)
WO (1) WO2010013805A1 (ja)

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS476780U (ja) * 1971-02-15 1972-09-22
JPS4969677A (ja) 1972-09-20 1974-07-05
JPH06310784A (ja) 1993-04-22 1994-11-04 Olympus Optical Co Ltd 半導体レーザの駆動装置
WO2005003131A1 (en) 2003-06-27 2005-01-13 Janssen Pharmaceutica N.V. Tricyclic delta opioid modulators
JP2008019121A (ja) 2006-07-12 2008-01-31 Babcock Hitachi Kk 水素製造装置
WO2008038711A1 (fr) * 2006-09-29 2008-04-03 Nippon Zoki Pharmaceutical Co., Ltd. Dérivé de l'oxépine

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR1502857A (fr) * 1965-10-01 1967-11-24 Sandoz Sa Nouveaux dérivés du benzo-cyclohepta-thiophène et leur préparation
CH531000A (de) * 1970-03-11 1972-11-30 Sandoz Ag Verfahren zur Herstellung neuer Benzocycloheptathiophene
CH568312A5 (ja) * 1972-01-24 1975-10-31 Sandoz Ag
JPS6310784A (ja) 1986-03-03 1988-01-18 Kyowa Hakko Kogyo Co Ltd 抗アレルギー剤
US4882351A (en) * 1987-10-14 1989-11-21 Roussel Uclaf Tricyclic compounds
JP3338913B2 (ja) * 1993-06-29 2002-10-28 大鵬薬品工業株式会社 テトラゾール誘導体
US6613905B1 (en) * 1998-01-21 2003-09-02 Millennium Pharmaceuticals, Inc. Chemokine receptor antagonists and methods of use therefor
ES2342110T3 (es) * 2005-06-17 2010-07-01 Janssen Pharmaceutica Nv Nuevos derivados tetraciclicos de tetrahidrofurano que contienen una cadena lateral de amina ciclica.
EP2243778B1 (en) * 2008-01-30 2014-10-29 Nippon Zoki Pharmaceutical Co., Ltd. Piperidine derivative

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS476780U (ja) * 1971-02-15 1972-09-22
JPS4969677A (ja) 1972-09-20 1974-07-05
JPH06310784A (ja) 1993-04-22 1994-11-04 Olympus Optical Co Ltd 半導体レーザの駆動装置
WO2005003131A1 (en) 2003-06-27 2005-01-13 Janssen Pharmaceutica N.V. Tricyclic delta opioid modulators
JP2008019121A (ja) 2006-07-12 2008-01-31 Babcock Hitachi Kk 水素製造装置
WO2008038711A1 (fr) * 2006-09-29 2008-04-03 Nippon Zoki Pharmaceutical Co., Ltd. Dérivé de l'oxépine

Non-Patent Citations (14)

* Cited by examiner, † Cited by third party
Title
COLLECT. CZECH. CHEM. COMMUM., vol. 59, 1994, pages 667 - 674
EMILE CHERBULIEZ, HELVETICA CHIMICA ACTA, 49, FASC., no. 26, 1966, pages 214 - 233
HELVETICA CHIMICA ACTA, 54, FASC, vol. 1, 1996, pages 214 - 233
HELVETICA CHIMICA ACTA, 54, FASC., vol. 1, 1971, pages 277 - 282
HELVETICA CHIMICA ACTA, 54, FASC., vol. 1, 1971, pages 277 - 283
HELVETICA CHIMICA ACTA, 59, FASC., vol. 3, 1976, pages 866 - 877
HELVETICA CHIMICA ACTA, vol. 49, no. 26, 1966, pages 214 - 233
HELVETICA CHIMICA ACTA, vol. 49, no. 26, 1966, pages 214 - 234
HELVETICA CHIMICAACTA, 54, FASC, vol. 1, no. 27, 1971, pages 7 - 282
J. AM. CHEM. SOC., vol. 124, 2002, pages 12557 - 12565
J. MED. CHEM., vol. 35, 1992, pages 2074 - 2084
J. ORG. CHEM., vol. 44, no. 22, 1979, pages 3760 - 3765
See also references of EP2319840A4
TETRAHEDRON LETT., vol. 40, 1991, pages 8193 - 8195

Also Published As

Publication number Publication date
TW201011038A (en) 2010-03-16
HK1206742A1 (en) 2016-01-15
DK2319840T3 (en) 2016-01-25
TWI457341B (zh) 2014-10-21
ES2561227T3 (es) 2016-02-25
KR20110049773A (ko) 2011-05-12
JP5379139B2 (ja) 2013-12-25
CN102112462B (zh) 2015-02-18
CN102112462A (zh) 2011-06-29
JPWO2010013805A1 (ja) 2012-01-12
CA2732282A1 (en) 2010-02-04
CN104693215A (zh) 2015-06-10
BRPI0917550A2 (pt) 2015-11-17
KR101375680B1 (ko) 2014-03-19
PT2319840E (pt) 2016-02-10
EP2319840A4 (en) 2012-05-16
PL2319840T3 (pl) 2016-03-31
AU2009277496B2 (en) 2013-09-26
JP2013253115A (ja) 2013-12-19
EP2319840B1 (en) 2015-12-16
JP5503793B2 (ja) 2014-05-28
CA2732282C (en) 2016-03-29
AU2009277496A1 (en) 2010-02-04
HK1159612A1 (en) 2012-09-21
CN104693215B (zh) 2017-09-01
US20110124856A1 (en) 2011-05-26
RU2483063C2 (ru) 2013-05-27
EP2319840A1 (en) 2011-05-11
RU2011107744A (ru) 2012-09-10
US8653285B2 (en) 2014-02-18

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