ES2454648T3 - Compuestos de 8-azabiciclo[3.2.1]octil-2-hidroxibenzamida como antagonistas de receptores opioides mu - Google Patents
Compuestos de 8-azabiciclo[3.2.1]octil-2-hidroxibenzamida como antagonistas de receptores opioides mu Download PDFInfo
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- ES2454648T3 ES2454648T3 ES08795602.5T ES08795602T ES2454648T3 ES 2454648 T3 ES2454648 T3 ES 2454648T3 ES 08795602 T ES08795602 T ES 08795602T ES 2454648 T3 ES2454648 T3 ES 2454648T3
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- oct
- alkyl
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- ethyl
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- 150000001875 compounds Chemical class 0.000 title claims abstract description 201
- 229940123257 Opioid receptor antagonist Drugs 0.000 title description 5
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- 125000001424 substituent group Chemical group 0.000 claims abstract description 16
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- 125000006652 (C3-C12) cycloalkyl group Chemical group 0.000 claims abstract description 14
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- 239000001509 sodium citrate Substances 0.000 description 1
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- BEOOHQFXGBMRKU-UHFFFAOYSA-N sodium cyanoborohydride Chemical compound [Na+].[B-]C#N BEOOHQFXGBMRKU-UHFFFAOYSA-N 0.000 description 1
- CSMWJXBSXGUPGY-UHFFFAOYSA-L sodium dithionate Chemical compound [Na+].[Na+].[O-]S(=O)(=O)S([O-])(=O)=O CSMWJXBSXGUPGY-UHFFFAOYSA-L 0.000 description 1
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- MENILFUADYEXNU-UHFFFAOYSA-N tert-butyl 3-oxo-8-azabicyclo[3.2.1]octane-8-carboxylate Chemical compound C1C(=O)CC2CCC1N2C(=O)OC(C)(C)C MENILFUADYEXNU-UHFFFAOYSA-N 0.000 description 1
- QHAKCMSTYYSRFT-UHFFFAOYSA-N tert-butyl n-(2-ethylbutyl)-n-(2-hydroxyethyl)carbamate Chemical compound CCC(CC)CN(CCO)C(=O)OC(C)(C)C QHAKCMSTYYSRFT-UHFFFAOYSA-N 0.000 description 1
- NYOOXIKIQAFNQY-UHFFFAOYSA-N tert-butyl n-(2-ethylbutyl)-n-(2-oxoethyl)carbamate Chemical compound CCC(CC)CN(CC=O)C(=O)OC(C)(C)C NYOOXIKIQAFNQY-UHFFFAOYSA-N 0.000 description 1
- AMUVUTCXNJBTPE-UHFFFAOYSA-N tert-butyl n-[(4,4-difluorocyclohexyl)methyl]-n-(2-hydroxyethyl)carbamate Chemical compound CC(C)(C)OC(=O)N(CCO)CC1CCC(F)(F)CC1 AMUVUTCXNJBTPE-UHFFFAOYSA-N 0.000 description 1
- HXBGEZFCNLSHPI-UHFFFAOYSA-N tert-butyl n-[(4,4-difluorocyclohexyl)methyl]-n-(2-oxoethyl)carbamate Chemical compound CC(C)(C)OC(=O)N(CC=O)CC1CCC(F)(F)CC1 HXBGEZFCNLSHPI-UHFFFAOYSA-N 0.000 description 1
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Classifications
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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
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- 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
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- 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
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- A—HUMAN NECESSITIES
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- 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
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- 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
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- 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
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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
- A61P25/04—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
Landscapes
- 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)
Applications Claiming Priority (5)
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| US966364P | 2007-08-27 | ||
| US5106508P | 2008-05-07 | 2008-05-07 | |
| US51065 | 2008-05-07 | ||
| PCT/US2008/010100 WO2009029256A1 (en) | 2007-08-27 | 2008-08-26 | 8-azabicyclo[3.2.1]octyl-2-hydroxybenzamide compounds as mu opioid receptor antagonists |
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| ES2454648T3 true ES2454648T3 (es) | 2014-04-11 |
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| 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) |
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| 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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| US6900228B1 (en) | 1998-03-10 | 2005-05-31 | Research Triangle Institute | Opiate compounds, methods of making and methods of use |
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| TWI244481B (en) | 1998-12-23 | 2005-12-01 | Pfizer | 3-azabicyclo[3.1.0]hexane derivatives useful in therapy |
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| CN101534827A (zh) | 2006-11-07 | 2009-09-16 | 尼克塔治疗亚拉巴马公司 | 阿片样物质激动剂和阿片样物质拮抗剂的剂型和联合给药 |
| 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 |
-
2008
- 2008-08-18 TW TW097131456A patent/TWI423801B/zh not_active IP Right Cessation
- 2008-08-26 US US12/229,664 patent/US7902220B2/en not_active Expired - Fee Related
- 2008-08-26 ES ES08795602.5T patent/ES2454648T3/es active Active
- 2008-08-26 JP JP2010522921A patent/JP5296078B2/ja not_active Expired - Fee Related
- 2008-08-26 EP EP08795602.5A patent/EP2183249B1/en not_active Not-in-force
- 2008-08-26 WO PCT/US2008/010100 patent/WO2009029256A1/en not_active Ceased
- 2008-08-26 CA CA2695755A patent/CA2695755C/en not_active Expired - Fee Related
- 2008-08-26 KR KR1020107006348A patent/KR101547214B1/ko not_active Expired - Fee Related
- 2008-08-26 AU AU2008293974A patent/AU2008293974B9/en not_active Ceased
- 2008-08-26 BR BRPI0815797-9A patent/BRPI0815797A2/pt not_active IP Right Cessation
- 2008-08-26 MX MX2010002171A patent/MX2010002171A/es active IP Right Grant
- 2008-08-26 CN CN2008801046626A patent/CN101790529B/zh not_active Expired - Fee Related
- 2008-08-27 AR ARP080103728A patent/AR068116A1/es unknown
-
2011
- 2011-01-26 US US13/014,012 patent/US8481563B2/en not_active Expired - Fee Related
-
2013
- 2013-06-10 US US13/914,093 patent/US8802698B2/en active Active
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2014
- 2014-06-26 US US14/315,582 patent/US9199993B2/en not_active Expired - Fee Related
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 |
| TWI423801B (zh) | 2014-01-21 |
| 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 |
| 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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