WO2008156102A1 - ピラゾロン誘導体及びそれらを有効成分とするｐｄｅ阻害剤 - Google Patents

ピラゾロン誘導体及びそれらを有効成分とするｐｄｅ阻害剤 Download PDF

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Publication number
WO2008156102A1
WO2008156102A1 PCT/JP2008/061104 JP2008061104W WO2008156102A1 WO 2008156102 A1 WO2008156102 A1 WO 2008156102A1 JP 2008061104 W JP2008061104 W JP 2008061104W WO 2008156102 A1 WO2008156102 A1 WO 2008156102A1
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WO
WIPO (PCT)
Prior art keywords
same
active ingredient
pyrazolone derivative
inhibitor containing
pde inhibitor
Prior art date
Application number
PCT/JP2008/061104
Other languages
English (en)
French (fr)
Inventor
Yasushi Kohno
Koji Ochiai
Satoshi Takita
Tetsuya Kishi
Original Assignee
Kyorin 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
Application filed by Kyorin Pharmaceutical Co., Ltd. filed Critical Kyorin Pharmaceutical Co., Ltd.
Priority to US12/452,173 priority Critical patent/US20100130738A1/en
Priority to JP2009520501A priority patent/JPWO2008156102A1/ja
Priority to CA002692249A priority patent/CA2692249A1/en
Priority to EP08777308A priority patent/EP2168960A1/en
Publication of WO2008156102A1 publication Critical patent/WO2008156102A1/ja

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    • 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
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P17/00—Drugs for dermatological disorders
    • 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
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    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P25/24—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
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • 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
    • 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
    • C07D405/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—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
    • C07D417/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems

Abstract

ホスホジエステラーゼ阻害作用を有する医薬品として有用な下記一般式（１）で表される新規ピラゾロン誘導体を提供すること。（１）　　Ｒ１，２：Ｃ１～６アルキル　 Ｒ３，４：Ｈ，Ｘ，Ｃ１～６アルコキシ　 Ｚ：Ｏ，Ｓ　 Ａ： AA, BB　（Ｒ５：Ｈ，Ｃ１～６アルキル；Ｒ６，７：Ｃ１～６アルキル）
PCT/JP2008/061104 2007-06-19 2008-06-18 ピラゾロン誘導体及びそれらを有効成分とするｐｄｅ阻害剤 WO2008156102A1 (ja)

Priority Applications (4)

Application Number Priority Date Filing Date Title
US12/452,173 US20100130738A1 (en) 2007-06-19 2008-06-18 Pyrazolone derivative and pde inhibitor containing the same as active ingredient
JP2009520501A JPWO2008156102A1 (ja) 2007-06-19 2008-06-18 ピラゾロン誘導体及びそれらを有効成分とするｐｄｅ阻害剤
CA002692249A CA2692249A1 (en) 2007-06-19 2008-06-18 Pyrazolone derivative and pde inhibitor containing the same as active ingredient
EP08777308A EP2168960A1 (en) 2007-06-19 2008-06-18 Pyrazolone derivative and pde inhibitor containing the same as active ingredient

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2007161195 2007-06-19
JP2007-161195 2007-06-19

Publications (1)

Publication Number Publication Date
WO2008156102A1 true WO2008156102A1 (ja) 2008-12-24

Family

ID=40156261

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/JP2008/061104 WO2008156102A1 (ja) 2007-06-19 2008-06-18 ピラゾロン誘導体及びそれらを有効成分とするｐｄｅ阻害剤

Country Status (5)

Country Link
US (1) US20100130738A1 (ja)
EP (1) EP2168960A1 (ja)
JP (1) JPWO2008156102A1 (ja)
CA (1) CA2692249A1 (ja)
WO (1) WO2008156102A1 (ja)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2012512192A (ja) * 2008-12-19 2012-05-31 レオ ファーマ アクティーゼルスカブ 皮膚疾患の処置のためのホスホジエステラーゼ阻害薬としてのトリアゾロピリジン誘導体
US8609848B2 (en) 2008-11-14 2013-12-17 Takeda Gmbh Pyrazolone-derivatives and their use as PDE-4 inhibitors
EP2719686A1 (en) * 2010-03-12 2014-04-16 Nippon Soda Co., Ltd. Process to halogenate a picoline derivative

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT2069312E (pt) * 2006-07-25 2013-01-24 Cephalon Inc Derivados de piridizinona
CN103664564B (zh) * 2012-09-06 2015-09-30 重庆博腾制药科技股份有限公司 一种镇痛药物中间体的制备方法
CN107001361A (zh) * 2014-12-02 2017-08-01 拜耳医药股份有限公司 杂芳基取代的咪唑并[1，2‑a]吡啶及其用途

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2007091597A (ja) * 2005-09-27 2007-04-12 Kyorin Pharmaceut Co Ltd ピラゾロピリジン−４−イルピラゾロン誘導体とその付加塩及びそれを有効成分とするホスホジエステラーゼ阻害剤
JP2007119397A (ja) * 2005-10-28 2007-05-17 Kyorin Pharmaceut Co Ltd ピラゾロピリジン誘導体とその付加塩及びそれらを有効成分とするｐｄｅ阻害剤
JP2008069144A (ja) * 2006-08-17 2008-03-27 Kyorin Pharmaceut Co Ltd ピラゾロン誘導体及びそれらを有効成分とするｐｄｅ阻害剤

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2007091597A (ja) * 2005-09-27 2007-04-12 Kyorin Pharmaceut Co Ltd ピラゾロピリジン−４−イルピラゾロン誘導体とその付加塩及びそれを有効成分とするホスホジエステラーゼ阻害剤
JP2007119397A (ja) * 2005-10-28 2007-05-17 Kyorin Pharmaceut Co Ltd ピラゾロピリジン誘導体とその付加塩及びそれらを有効成分とするｐｄｅ阻害剤
JP2008069144A (ja) * 2006-08-17 2008-03-27 Kyorin Pharmaceut Co Ltd ピラゾロン誘導体及びそれらを有効成分とするｐｄｅ阻害剤

Cited By (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8609848B2 (en) 2008-11-14 2013-12-17 Takeda Gmbh Pyrazolone-derivatives and their use as PDE-4 inhibitors
US9340522B2 (en) 2008-11-14 2016-05-17 Takeda Gmbh Pyrazolone-derivatives and their use as PDE-4 inhibitors
JP2012512192A (ja) * 2008-12-19 2012-05-31 レオ ファーマ アクティーゼルスカブ 皮膚疾患の処置のためのホスホジエステラーゼ阻害薬としてのトリアゾロピリジン誘導体
EP2719686A1 (en) * 2010-03-12 2014-04-16 Nippon Soda Co., Ltd. Process to halogenate a picoline derivative
US8841458B2 (en) 2010-03-12 2014-09-23 Nippon Soda Co., Ltd. Compound containing pyridine ring and method for producing halogenated picoline derivative and tetrazolyloxime derivative
US8962848B2 (en) 2010-03-12 2015-02-24 Nippon Soda Co., Ltd. Compound containing pyridine ring and method for producing halogenated picoline derivative and tetrazolyloxime derivative
US9000178B2 (en) 2010-03-12 2015-04-07 Nippon Soda Co., Ltd. Compound containing pyridine ring and method for producing halogenated picoline derivative and tetrazolyloxime derivative
US9012653B2 (en) 2010-03-12 2015-04-21 Nippon Soda Co., Ltd. Compound containing pyridine ring and method for producing halogenated picoline derivative and tetrazolyloxime derivative
US9018385B2 (en) 2010-03-12 2015-04-28 Nippon Soda Co., Ltd. Compound containing pyridine ring and method for producing halogenated picoline derivative and tetrazolyloxime derivative

Also Published As

Publication number Publication date
CA2692249A1 (en) 2008-12-24
US20100130738A1 (en) 2010-05-27
JPWO2008156102A1 (ja) 2010-08-26
EP2168960A1 (en) 2010-03-31

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