TWI423801B - 作為μ類鴉片受體拮抗劑之８－氮雜雙環〔３．２．１〕辛基－２－羥基苯甲醯胺化合物 - Google Patents

作為μ類鴉片受體拮抗劑之８－氮雜雙環〔３．２．１〕辛基－２－羥基苯甲醯胺化合物 Download PDF

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Publication number
TWI423801B
TWI423801B TW097131456A TW97131456A TWI423801B TW I423801 B TWI423801 B TW I423801B TW 097131456 A TW097131456 A TW 097131456A TW 97131456 A TW97131456 A TW 97131456A TW I423801 B TWI423801 B TW I423801B
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TW
Taiwan
Prior art keywords
compound
oct
alkyl
ethyl
azabicyclo
Prior art date
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TW097131456A
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English (en)
Chinese (zh)
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TW200918057A (en
Inventor
Daisuke Roland Saito
Daniel D Long
Priscilla Vandyke
Timothy J Church
Lan Jiang
Bryan Frieman
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Theravance Inc
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Publication of TW200918057A publication Critical patent/TW200918057A/zh
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Publication of TWI423801B publication Critical patent/TWI423801B/zh

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    • 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
    • C07D471/08—Bridged 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
    • A61K31/46—8-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, cocaine
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/485—Morphinan derivatives, e.g. morphine, codeine
    • 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
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/10—Laxatives
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Emergency Medicine (AREA)
  • Epidemiology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Otolaryngology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
TW097131456A 2007-08-27 2008-08-18 作為μ類鴉片受體拮抗劑之８－氮雜雙環〔３．２．１〕辛基－２－羥基苯甲醯胺化合物 TWI423801B (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US96636407P 2007-08-27 2007-08-27
US5106508P 2008-05-07 2008-05-07

Publications (2)

Publication Number Publication Date
TW200918057A TW200918057A (en) 2009-05-01
TWI423801B true TWI423801B (zh) 2014-01-21

Family

ID=40042620

Family Applications (1)

Application Number Title Priority Date Filing Date
TW097131456A TWI423801B (zh) 2007-08-27 2008-08-18 作為μ類鴉片受體拮抗劑之８－氮雜雙環〔３．２．１〕辛基－２－羥基苯甲醯胺化合物

Country Status (13)

Country Link
US (4) US7902220B2 (enExample)
EP (1) EP2183249B1 (enExample)
JP (1) JP5296078B2 (enExample)
KR (1) KR101547214B1 (enExample)
CN (1) CN101790529B (enExample)
AR (1) AR068116A1 (enExample)
AU (1) AU2008293974B9 (enExample)
BR (1) BRPI0815797A2 (enExample)
CA (1) CA2695755C (enExample)
ES (1) ES2454648T3 (enExample)
MX (1) MX2010002171A (enExample)
TW (1) TWI423801B (enExample)
WO (1) WO2009029256A1 (enExample)

Families Citing this family (14)

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MY145633A (en) 2006-03-01 2012-03-15 Theravance Inc 8-azabicyclo[3.2.1]octane compounds as mu opioid receptor antagonists
TWI415850B (zh) * 2007-07-20 2013-11-21 Theravance Inc 製備ｍｕ類鴉片受體拮抗劑之中間物的方法
EP2185553B1 (en) * 2007-08-27 2012-06-27 Theravance, Inc. Amidoalkyl-8-azabicyclo[3.2.1]octane compounds as mu opioid receptor antagonists
EP2195313B1 (en) * 2007-08-27 2014-04-02 Theravance, Inc. Heteroarylalkyl-8-azabicyclo[3.2.1]octane compounds as mu opioid receptor antagonists
TWI423801B (zh) 2007-08-27 2014-01-21 Theravance Inc 作為μ類鴉片受體拮抗劑之８－氮雜雙環〔３．２．１〕辛基－２－羥基苯甲醯胺化合物
ES2364686T3 (es) * 2007-08-27 2011-09-12 Theravance, Inc. Compuestos de alquil-8-azabiciclo[3.2.1]octano disustituidos como antagonistas del receptor opioide mu.
AR080056A1 (es) 2010-02-01 2012-03-07 Novartis Ag Derivados de ciclohexil-amida como antagonistas de los receptores de crf
JP2013518085A (ja) 2010-02-01 2013-05-20 ノバルティス アーゲー ＣＲＦ−１受容体アンタゴニストとしてのピラゾロ［５，１ｂ］オキサゾール誘導体
US8835444B2 (en) 2010-02-02 2014-09-16 Novartis Ag Cyclohexyl amide derivatives as CRF receptor antagonists
WO2018159716A1 (ja) * 2017-03-02 2018-09-07 株式会社 三和化学研究所 アルコール使用障害の治療薬
JP7197880B2 (ja) * 2017-10-19 2022-12-28 学校法人 名城大学 エステル化剤及びその利用
JP2021512952A (ja) 2018-02-05 2021-05-20 アルカームス・インコーポレイテッド 疼痛の処置のための化合物
CN108732292B (zh) * 2018-04-27 2020-07-14 中国人民解放军第二军医大学 血浆中舒芬太尼的快速检测方法及装置
US20220348572A1 (en) * 2019-08-09 2022-11-03 The National Institutes of Pharmaceutical R&D Co., Ltd. Bridged heterocyclyl-substituted pyrimidine compound, preparation method therefor, and pharmaceutical use thereof

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WO2004089908A2 (en) * 2003-04-14 2004-10-21 Pfizer Products Inc. 3-azabicyclo[3.2.1]octane derivatives
WO2004089909A1 (en) * 2003-04-14 2004-10-21 Pfizer Products Inc. 2-azabicyclo[3.3.1]nonane derivatives as opioid receptor antagonists

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US20020025948A1 (en) 2000-06-23 2002-02-28 Banks Bernard Joseph 3-azabicyclo[3.1.0]hexane derivatives useful in therapy
EA006708B1 (ru) 2001-10-22 2006-02-24 Пфайзер Продактс Инк. Производные 3-азабицикло (3.1.0) гексана в качестве антагонистов опиоидного рецептора
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MY145633A (en) 2006-03-01 2012-03-15 Theravance Inc 8-azabicyclo[3.2.1]octane compounds as mu opioid receptor antagonists
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TWI409067B (zh) 2007-02-28 2013-09-21 Theravance Inc ８-氮雜雙環〔３．２．１〕辛烷化合物之結晶型
TWI415850B (zh) 2007-07-20 2013-11-21 Theravance Inc 製備ｍｕ類鴉片受體拮抗劑之中間物的方法
ES2364686T3 (es) 2007-08-27 2011-09-12 Theravance, Inc. Compuestos de alquil-8-azabiciclo[3.2.1]octano disustituidos como antagonistas del receptor opioide mu.
EP2185553B1 (en) 2007-08-27 2012-06-27 Theravance, Inc. Amidoalkyl-8-azabicyclo[3.2.1]octane compounds as mu opioid receptor antagonists
EP2195313B1 (en) * 2007-08-27 2014-04-02 Theravance, Inc. Heteroarylalkyl-8-azabicyclo[3.2.1]octane compounds as mu opioid receptor antagonists
TWI423801B (zh) 2007-08-27 2014-01-21 Theravance Inc 作為μ類鴉片受體拮抗劑之８－氮雜雙環〔３．２．１〕辛基－２－羥基苯甲醯胺化合物

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Also Published As

Publication number Publication date
US20110118306A1 (en) 2011-05-19
US9199993B2 (en) 2015-12-01
US20150051243A1 (en) 2015-02-19
EP2183249A1 (en) 2010-05-12
US20090062333A1 (en) 2009-03-05
US7902220B2 (en) 2011-03-08
CA2695755A1 (en) 2009-03-05
BRPI0815797A2 (pt) 2015-06-16
AU2008293974B2 (en) 2013-09-05
JP2010537978A (ja) 2010-12-09
EP2183249B1 (en) 2014-02-26
MX2010002171A (es) 2010-04-30
CN101790529A (zh) 2010-07-28
ES2454648T3 (es) 2014-04-11
CA2695755C (en) 2016-08-09
CN101790529B (zh) 2012-09-05
US20140080855A1 (en) 2014-03-20
US8802698B2 (en) 2014-08-12
JP5296078B2 (ja) 2013-09-25
US8481563B2 (en) 2013-07-09
AR068116A1 (es) 2009-11-04
WO2009029256A1 (en) 2009-03-05
KR20100045524A (ko) 2010-05-03
TW200918057A (en) 2009-05-01
AU2008293974A1 (en) 2009-03-05
AU2008293974B9 (en) 2013-10-31
KR101547214B1 (ko) 2015-08-25

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