WO2009063953A1 - フェニルピラゾール誘導体 - Google Patents

フェニルピラゾール誘導体 Download PDF

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Publication number
WO2009063953A1
WO2009063953A1 PCT/JP2008/070712 JP2008070712W WO2009063953A1 WO 2009063953 A1 WO2009063953 A1 WO 2009063953A1 JP 2008070712 W JP2008070712 W JP 2008070712W WO 2009063953 A1 WO2009063953 A1 WO 2009063953A1
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WO
WIPO (PCT)
Prior art keywords
alkyl
disorder
halogeno
general formula
sleep
Prior art date
Application number
PCT/JP2008/070712
Other languages
English (en)
French (fr)
Inventor
Toshio Nakamura
Makoto Tatsuzuki
Dai Nozawa
Tomoko Tamita
Seiji Masuda
Hiroshi Ohta
Shuhei Kashiwa
Aya Fujino
Shigeyuki Chaki
Toshiharu Shimazaki
Original Assignee
Taisho Pharmaceutical Co., Ltd.
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 SI200831096T priority Critical patent/SI2221298T1/sl
Priority to AU2008321823A priority patent/AU2008321823B2/en
Priority to EP08849725.0A priority patent/EP2221298B1/en
Priority to CN200880115707XA priority patent/CN101855211B/zh
Priority to ES08849725T priority patent/ES2436146T3/es
Priority to BRPI0820432A priority patent/BRPI0820432B8/pt
Priority to MX2010005225A priority patent/MX2010005225A/es
Priority to PL08849725T priority patent/PL2221298T3/pl
Priority to CA2705502A priority patent/CA2705502C/en
Priority to US12/741,754 priority patent/US7888354B2/en
Priority to RS20130586A priority patent/RS53125B/en
Priority to NZ585661A priority patent/NZ585661A/en
Priority to DK08849725.0T priority patent/DK2221298T3/da
Priority to RU2010123924/04A priority patent/RU2480456C2/ru
Application filed by Taisho Pharmaceutical Co., Ltd. filed Critical Taisho Pharmaceutical Co., Ltd.
Priority to JP2009541174A priority patent/JP4543344B2/ja
Publication of WO2009063953A1 publication Critical patent/WO2009063953A1/ja
Priority to IL205509A priority patent/IL205509A/en
Priority to ZA2010/03111A priority patent/ZA201003111B/en
Priority to US12/951,964 priority patent/US8183387B2/en
Priority to US12/951,978 priority patent/US8193176B2/en
Priority to HK10112206.3A priority patent/HK1145834A1/xx
Priority to HRP20131060AT priority patent/HRP20131060T1/hr
Priority to IL236083A priority patent/IL236083A/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/20—Hypnotics; Sedatives
    • 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
    • A61P25/24—Antidepressants
    • 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
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D231/38—Nitrogen atoms
    • C07D231/40—Acylated on said nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • C07D401/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

Abstract

　認知症、アルツハイマー病、注意欠陥・多動性症、統合失調症、摂食障害、肥満、糖尿病、高脂血症、睡眠障害、ナルコレプシー、睡眠時無呼吸症候群、概日リズム障害、うつ病、又はアレルギー性鼻炎等の疾患の予防又は治療薬を提供すること。 式（１） ｛式（１）中、 Ｒ1及びＲ2は、同一又は異なって、Ｃ1～Ｃ6アルキル若しくはＣ3～Ｃ8環状アルキルを示し、 又は、Ｒ1及びＲ2は、隣接する窒素原子と一緒になって互いに結合した４～７員の飽和複素環（該飽和複素環基は、ハロゲン又はＣ1～Ｃ6アルキルで置換されても良い）を形成し、 ｎは、０～２の整数を示し、 Ｔは、水素原子；ハロゲン又はＣ1～Ｃ6アルキルを示し、Ｒは式（Ｉ） 等を示す。｝ で表されるフェニルピラゾール誘導体、又はその医薬上許容される塩。
PCT/JP2008/070712 2007-11-13 2008-11-13 フェニルピラゾール誘導体 WO2009063953A1 (ja)

Priority Applications (22)

Application Number Priority Date Filing Date Title
RS20130586A RS53125B (en) 2007-11-13 2008-11-13 Phenylpyrazole derivatives
EP08849725.0A EP2221298B1 (en) 2007-11-13 2008-11-13 Phenylpyrazole derivatives
CN200880115707XA CN101855211B (zh) 2007-11-13 2008-11-13 苯基吡唑衍生物
ES08849725T ES2436146T3 (es) 2007-11-13 2008-11-13 Derivados de fenilpirazol
BRPI0820432A BRPI0820432B8 (pt) 2007-11-13 2008-11-13 derivados de fenilpirazol apresentando atividade de antagonista de receptor de histamina h3 e um agente profilático ou terapeutico compreendendo tais derivados
MX2010005225A MX2010005225A (es) 2007-11-13 2008-11-13 Derivados de fenilpirazol.
PL08849725T PL2221298T3 (pl) 2007-11-13 2008-11-13 Pochodne fenylopirazolu
CA2705502A CA2705502C (en) 2007-11-13 2008-11-13 Phenylpyrazole derivatives
AU2008321823A AU2008321823B2 (en) 2007-11-13 2008-11-13 Phenylpyrazole derivatives
NZ585661A NZ585661A (en) 2007-11-13 2008-11-13 Phenylpyrazole derivatives
US12/741,754 US7888354B2 (en) 2007-11-13 2008-11-13 Phenylpyrazole derivatives
SI200831096T SI2221298T1 (sl) 2007-11-13 2008-11-13 Derivati fenilpirazola
RU2010123924/04A RU2480456C2 (ru) 2007-11-13 2008-11-13 Фенилпиразольные производные
DK08849725.0T DK2221298T3 (da) 2007-11-13 2008-11-13 Phenylpyrazolderivater
JP2009541174A JP4543344B2 (ja) 2007-11-13 2008-11-13 フェニルピラゾール誘導体
IL205509A IL205509A (en) 2007-11-13 2010-05-03 Phenyl-pyrazole derivatives
ZA2010/03111A ZA201003111B (en) 2007-11-13 2010-05-04 Phenylpyrazole derivatives
US12/951,964 US8183387B2 (en) 2007-11-13 2010-11-22 Phenylpyrazole derivatives
US12/951,978 US8193176B2 (en) 2007-11-13 2010-11-22 Phenylpyrazole derivatives
HK10112206.3A HK1145834A1 (en) 2007-11-13 2010-12-29 Phenylpyrazole derivatives
HRP20131060AT HRP20131060T1 (hr) 2007-11-13 2013-11-07 Derivati fenilpirazola
IL236083A IL236083A (en) 2007-11-13 2014-12-04 Phenyl-pyrazole derivatives

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
JP2007-294040 2007-11-13
JP2007294040 2007-11-13
JP2008-153736 2008-06-12
JP2008153736 2008-06-12

Related Child Applications (3)

Application Number Title Priority Date Filing Date
US12/741,754 A-371-Of-International US7888354B2 (en) 2007-11-13 2008-11-13 Phenylpyrazole derivatives
US12/951,964 Division US8183387B2 (en) 2007-11-13 2010-11-22 Phenylpyrazole derivatives
US12/951,978 Division US8193176B2 (en) 2007-11-13 2010-11-22 Phenylpyrazole derivatives

Publications (1)

Publication Number Publication Date
WO2009063953A1 true WO2009063953A1 (ja) 2009-05-22

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Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/JP2008/070712 WO2009063953A1 (ja) 2007-11-13 2008-11-13 フェニルピラゾール誘導体

Country Status (24)

Country Link
US (3) US7888354B2 (ja)
EP (1) EP2221298B1 (ja)
JP (2) JP4543344B2 (ja)
KR (1) KR101571176B1 (ja)
CN (1) CN101855211B (ja)
AU (1) AU2008321823B2 (ja)
BR (1) BRPI0820432B8 (ja)
CA (1) CA2705502C (ja)
CY (1) CY1114877T1 (ja)
DK (1) DK2221298T3 (ja)
ES (1) ES2436146T3 (ja)
HK (1) HK1145834A1 (ja)
HR (1) HRP20131060T1 (ja)
IL (2) IL205509A (ja)
MX (1) MX2010005225A (ja)
MY (1) MY173546A (ja)
NZ (1) NZ585661A (ja)
PL (1) PL2221298T3 (ja)
PT (1) PT2221298E (ja)
RS (1) RS53125B (ja)
RU (1) RU2480456C2 (ja)
SI (1) SI2221298T1 (ja)
WO (1) WO2009063953A1 (ja)
ZA (1) ZA201003111B (ja)

Cited By (6)

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Publication number Priority date Publication date Assignee Title
WO2013085018A1 (ja) 2011-12-08 2013-06-13 大正製薬株式会社 フェニルピロール誘導体
WO2013100054A1 (ja) 2011-12-27 2013-07-04 大正製薬株式会社 フェニルトリアゾール誘導体
WO2013151982A1 (en) 2012-04-03 2013-10-10 Arena Pharmaceuticals, Inc. Methods and compounds useful in treating pruritus, and methods for identifying such compounds
JP2016501246A (ja) * 2012-12-07 2016-01-18 ケモセントリックス，インコーポレイティド ジアゾールラクタム
JP2016506910A (ja) * 2013-01-17 2016-03-07 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ Ｃｎｓ疾患の処置のためのオキシトシン受容体アゴニスト
US10568870B2 (en) 2016-04-07 2020-02-25 Chemocentryx, Inc. Reducing tumor burden by administering CCR1 antagonists in combination with PD-1 inhibitors or PD-L1 inhibitors

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US20100113776A1 (en) * 2006-12-14 2010-05-06 Taisho Pharmaceutical Co.,Ltd. Pyrazole derivative
KR101571176B1 (ko) * 2007-11-13 2015-11-23 다이쇼 세이야꾸 가부시끼가이샤 페닐피라졸 유도체
JP5740838B2 (ja) * 2009-05-12 2015-07-01 大正製薬株式会社 フェニルピラゾール誘導体

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WO2013085018A1 (ja) 2011-12-08 2013-06-13 大正製薬株式会社 フェニルピロール誘導体
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