WO2008096870A1 - アザ架橋環化合物 - Google Patents

アザ架橋環化合物 Download PDF

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Publication number
WO2008096870A1
WO2008096870A1 PCT/JP2008/052189 JP2008052189W WO2008096870A1 WO 2008096870 A1 WO2008096870 A1 WO 2008096870A1 JP 2008052189 W JP2008052189 W JP 2008052189W WO 2008096870 A1 WO2008096870 A1 WO 2008096870A1
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WIPO (PCT)
Prior art keywords
aza
bridged
muscarinic
receptor
antagonistic activity
Prior art date
Application number
PCT/JP2008/052189
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English (en)
French (fr)
Inventor
Shinya Nagashima
Toru Kontani
Hiroshi Nagata
Yuji Matsushima
Hisao Hamaguchi
Tadatsura Koshika
Original Assignee
Astellas Pharma Inc.
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 Astellas Pharma Inc. filed Critical Astellas Pharma Inc.
Priority to KR1020097018755A priority Critical patent/KR20090107567A/ko
Priority to CA002678193A priority patent/CA2678193A1/en
Priority to JP2008557177A priority patent/JP5293192B2/ja
Priority to EP08711068A priority patent/EP2119716A4/en
Priority to US12/524,758 priority patent/US8367696B2/en
Priority to AU2008212171A priority patent/AU2008212171A1/en
Priority to MX2009008509A priority patent/MX2009008509A/es
Priority to CN2008800044089A priority patent/CN101605784B/zh
Priority to BRPI0806972-7A2A priority patent/BRPI0806972A2/pt
Publication of WO2008096870A1 publication Critical patent/WO2008096870A1/ja
Priority to IL200152A priority patent/IL200152A0/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
    • C07D453/02—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/439—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/06—Anti-spasmodics, e.g. drugs for colics, esophagic dyskinesia
    • 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
    • A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • 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
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/10—Drugs for disorders of the urinary system of the bladder
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/16—Otologicals
    • 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
    • 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
    • A61P3/08—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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07D471/12—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 three hetero rings
    • C07D471/18—Bridged systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Pulmonology (AREA)
  • Obesity (AREA)
  • Pain & Pain Management (AREA)
  • Hematology (AREA)
  • Biomedical Technology (AREA)
  • Otolaryngology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Epidemiology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

【課題】ムスカリンM3 受容体拮抗作用を有し、慢性閉塞性肺疾患(COPD)や喘息などの炎症性疾患の予防及び／または治療剤の有効成分として有用な化合物を提供する。【解決手段】本発明者らは、ムスカリンM3 受容体結合拮抗作用を有する化合物について検討し、下記式（１）のアザ架橋環化合物またはその塩がムスカリンM3 受容体結合拮抗作用を有することを確認し、本発明を完成した。本発明のアザ架橋環化合物はムスカリンM3 受容体結合拮抗作用を有し、慢性閉塞性肺疾患(COPD)や喘息等の炎症性疾患の予防及び／または治療剤として使用することができる。［R1 は、-H またはC1-6 アルキル；R2 は、式(a)，(b)，(c)および(d)からなる群より選択されるアザ架橋環であり；R3 は、チエニル、フェニル、ピリジル、ピラジニル、チアゾリル、またはピラゾリル；である］
PCT/JP2008/052189 2007-02-09 2008-02-08 アザ架橋環化合物 WO2008096870A1 (ja)

Priority Applications (10)

Application Number Priority Date Filing Date Title
KR1020097018755A KR20090107567A (ko) 2007-02-09 2008-02-08 아자 가교환 화합물
CA002678193A CA2678193A1 (en) 2007-02-09 2008-02-08 Aza-bridged-ring compound
JP2008557177A JP5293192B2 (ja) 2007-02-09 2008-02-08 アザ架橋環化合物
EP08711068A EP2119716A4 (en) 2007-02-09 2008-02-08 AZA BRIDGE CYCLE COMPOUND
US12/524,758 US8367696B2 (en) 2007-02-09 2008-02-08 Aza-bridged-ring compound
AU2008212171A AU2008212171A1 (en) 2007-02-09 2008-02-08 Aza-bridged-ring compound
MX2009008509A MX2009008509A (es) 2007-02-09 2008-02-08 Compuesto de anillo puenteado-aza.
CN2008800044089A CN101605784B (zh) 2007-02-09 2008-02-08 氮杂桥环化合物
BRPI0806972-7A2A BRPI0806972A2 (pt) 2007-02-09 2008-02-08 Composto cíclico contendo ponte azo
IL200152A IL200152A0 (en) 2007-02-09 2009-07-30 Aza-bridged-ring compound

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2007-030963 2007-02-09
JP2007030963 2007-02-09

Publications (1)

Publication Number Publication Date
WO2008096870A1 true WO2008096870A1 (ja) 2008-08-14

Family

ID=39681769

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/JP2008/052189 WO2008096870A1 (ja) 2007-02-09 2008-02-08 アザ架橋環化合物

Country Status (12)

Country Link
US (1) US8367696B2 (ja)
EP (1) EP2119716A4 (ja)
JP (1) JP5293192B2 (ja)
KR (1) KR20090107567A (ja)
CN (1) CN101605784B (ja)
AU (1) AU2008212171A1 (ja)
BR (1) BRPI0806972A2 (ja)
CA (1) CA2678193A1 (ja)
IL (1) IL200152A0 (ja)
MX (1) MX2009008509A (ja)
RU (1) RU2441868C2 (ja)
WO (1) WO2008096870A1 (ja)

Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8314119B2 (en) 2006-11-06 2012-11-20 Abbvie Inc. Azaadamantane derivatives and methods of use
WO2014051055A1 (ja) * 2012-09-28 2014-04-03 東レ株式会社 キヌクリジンウレア誘導体及びその医薬用途
JP2015527406A (ja) * 2012-09-11 2015-09-17 ジェンザイム・コーポレーション グルコシルセラミド合成酵素阻害剤
JP2016525571A (ja) * 2013-07-30 2016-08-25 ドン−ア エスティ カンパニー リミテッド 新規なビフェニル誘導体及びその製造方法
JP2016528199A (ja) * 2013-07-13 2016-09-15 ベイジン エフエスウェルカム テクノロジー ディベロップメント カンパニー リミテッド キニン系化合物、その光学異性体及びその製造方法と医薬用途
US9464078B2 (en) 2010-09-23 2016-10-11 Abbvie Inc. Monohydrate of azaadamantane derivatives
WO2017114377A1 (zh) * 2015-12-29 2017-07-06 四川海思科制药有限公司 一种苯基杂环衍生物及其在医药上的用途

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CA2679870A1 (en) * 2007-03-23 2008-10-02 Abbott Laboratories Azaadamantane ester and carbamate derivatives and methods of use thereof
SG11201901431PA (en) 2016-08-26 2019-03-28 Dong A St Co Ltd Novel salt of (r)-(1-methylpyrrolidine-3-yl)methyl(3'-chloro-4'-fluoro-[1,1'-biphenyl]-2-yl)carbamate and a crystal form thereof
KR102239776B1 (ko) * 2016-08-26 2021-04-13 동아에스티 주식회사 (r)-(1-메틸피롤리딘-3-일)메틸(3'-클로로-4'-플루오로-[1,1'-비페닐]-2-일)카바메이트의 신규염 및 이의 결정형
WO2019096226A1 (en) 2017-11-16 2019-05-23 Chengdu Easton Biopharmaceuticals Co., Ltd. Pasylated vegfr/pdgfr fusion proteins and their use in therapy
JP2021505569A (ja) 2017-12-04 2021-02-18 フリードリヒ−アレクサンダー−ウニヴェルシテート エアランゲン−ニュルンベルク Ｍ２よりもｍ３に対して選択性を有するフルオロフェニル置換ムスカリン受容体リガンド
EP4185267A1 (en) 2020-07-24 2023-05-31 Genzyme Corporation Pharmaceutical compositions comprising venglustat

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US5834499A (en) 1994-03-11 1998-11-10 Yamanouchi Pharmaceutical Co., Ltd. 5-HT3 receptor agonist, novel thiazole derivative and intermediate thereof
JPH08198751A (ja) * 1995-01-19 1996-08-06 Yamanouchi Pharmaceut Co Ltd カルバメート誘導体
JP2001521033A (ja) 1997-10-29 2001-11-06 スミスクライン・ビーチャム・パブリック・リミテッド・カンパニー 抗菌物質としてのプレウロムチリン誘導体
JP2003516391A (ja) * 1999-12-07 2003-05-13 セラヴァンス インコーポレーテッド ムスカリン性レセプターアンタゴニスト活性を有するウレア化合物
JP2004530641A (ja) * 2000-12-22 2004-10-07 アルミラル・プロデスフアルマ・アクチエンゲゼルシヤフト キヌクリジンカルバメート誘導体およびｍ３アンダゴニストとしてのそれらの使用

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Cited By (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8314119B2 (en) 2006-11-06 2012-11-20 Abbvie Inc. Azaadamantane derivatives and methods of use
US8987453B2 (en) 2006-11-06 2015-03-24 Abbvie Inc. Azaadamantane derivatives and methods of use
US9464078B2 (en) 2010-09-23 2016-10-11 Abbvie Inc. Monohydrate of azaadamantane derivatives
JP2015527406A (ja) * 2012-09-11 2015-09-17 ジェンザイム・コーポレーション グルコシルセラミド合成酵素阻害剤
WO2014051055A1 (ja) * 2012-09-28 2014-04-03 東レ株式会社 キヌクリジンウレア誘導体及びその医薬用途
JP2016528199A (ja) * 2013-07-13 2016-09-15 ベイジン エフエスウェルカム テクノロジー ディベロップメント カンパニー リミテッド キニン系化合物、その光学異性体及びその製造方法と医薬用途
JP2016525571A (ja) * 2013-07-30 2016-08-25 ドン−ア エスティ カンパニー リミテッド 新規なビフェニル誘導体及びその製造方法
WO2017114377A1 (zh) * 2015-12-29 2017-07-06 四川海思科制药有限公司 一种苯基杂环衍生物及其在医药上的用途

Also Published As

Publication number Publication date
KR20090107567A (ko) 2009-10-13
RU2009133781A (ru) 2011-03-20
CA2678193A1 (en) 2008-08-14
AU2008212171A1 (en) 2008-08-14
EP2119716A1 (en) 2009-11-18
CN101605784B (zh) 2013-04-10
MX2009008509A (es) 2009-08-20
US20100105658A1 (en) 2010-04-29
RU2441868C2 (ru) 2012-02-10
JPWO2008096870A1 (ja) 2010-05-27
CN101605784A (zh) 2009-12-16
BRPI0806972A2 (pt) 2014-04-08
JP5293192B2 (ja) 2013-09-18
IL200152A0 (en) 2010-04-15
US8367696B2 (en) 2013-02-05
EP2119716A4 (en) 2011-06-01

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