TWI685497B - 具有多重模式抗疼痛活性的１-氧雜-４,９-二氮雜螺十一烷化合物之烷基衍生物 - Google Patents
具有多重模式抗疼痛活性的１-氧雜-４,９-二氮雜螺十一烷化合物之烷基衍生物 Download PDFInfo
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- TWI685497B TWI685497B TW104117583A TW104117583A TWI685497B TW I685497 B TWI685497 B TW I685497B TW 104117583 A TW104117583 A TW 104117583A TW 104117583 A TW104117583 A TW 104117583A TW I685497 B TWI685497 B TW I685497B
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- Prior art keywords
- oxa
- unsubstituted
- substituted
- ethyl
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- 208000002193 Pain Diseases 0.000 title claims abstract description 64
- 230000036407 pain Effects 0.000 title claims abstract description 47
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- 229960001367 tartaric acid Drugs 0.000 description 1
- 235000002906 tartaric acid Nutrition 0.000 description 1
- RCINICONZNJXQF-MZXODVADSA-N taxol Chemical compound O([C@@H]1[C@@]2(C[C@@H](C(C)=C(C2(C)C)[C@H](C([C@]2(C)[C@@H](O)C[C@H]3OC[C@]3([C@H]21)OC(C)=O)=O)OC(=O)C)OC(=O)[C@H](O)[C@@H](NC(=O)C=1C=CC=CC=1)C=1C=CC=CC=1)O)C(=O)C1=CC=CC=C1 RCINICONZNJXQF-MZXODVADSA-N 0.000 description 1
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- 238000011200 topical administration Methods 0.000 description 1
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- QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 description 1
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Classifications
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- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/537—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines spiro-condensed or forming part of bridged 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5386—1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/10—Spiro-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Pain & Pain Management (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
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| EP14382209 | 2014-06-02 | ||
| EP14382209.6 | 2014-06-02 |
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| TW201617352A TW201617352A (zh) | 2016-05-16 |
| TWI685497B true TWI685497B (zh) | 2020-02-21 |
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| TW201615643A (zh) | 2014-06-02 | 2016-05-01 | 伊史帝夫博士實驗室股份有限公司 | 具有多重模式抗疼痛活性之１－氧雜－４，９－二氮雜螺十一烷化合物之烷基與芳基衍生物 |
| AR106444A1 (es) * | 2015-10-23 | 2018-01-17 | Esteve Labor Dr | Compuestos oxaazaespíricos con actividad contra el dolor |
| RS59956B1 (sr) | 2015-10-23 | 2020-03-31 | Esteve Pharmaceuticals Sa | Oksa-diazaspiro jedinjenja koja imaju aktivnost protiv bola |
| TN2018000122A1 (en) * | 2015-11-16 | 2019-10-04 | Esteve Labor Dr | Oxadiazaspiro compounds for the treatment of drug abuse and addiction |
| US10807970B2 (en) * | 2016-05-20 | 2020-10-20 | Esteve Pharmaceuticals, S.A. | Tetrahydropyran and thiopyran derivatives having multimodal activity against pain |
| FI3697795T3 (fi) * | 2017-10-17 | 2024-02-23 | Acondicionamiento Tarrasense | (R)-9-(2,5-difluorifenetyyli)-4-etyyli-2-metyyli-1-oksa-4,9-diatsaspiro[5.5]undekan-3-onin suoloja |
| WO2019158634A1 (en) | 2018-02-16 | 2019-08-22 | Esteve Pharmaceuticals, S.A. | Deuterated derivatives of 9-(2,5-difluorophenethyl)-4-ethyl-2-methyl-1-oxa-4,9-diazaspiro[5.5]undecan-3-one |
| WO2019180188A1 (en) * | 2018-03-23 | 2019-09-26 | Esteve Pharmaceuticals, S.A. | Aminopropoxyphenyl and benzyl 1-oxa-4,9-diazaspiroundecane derivatives having multimodal activity against pain |
| WO2020157026A1 (en) * | 2019-01-28 | 2020-08-06 | Esteve Pharmaceuticals, S.A. | Hydroxylated derivatives of 1-oxa-4,9-diazaspiro undecane compounds having multimodal activity against pain |
| WO2021018824A1 (en) | 2019-07-31 | 2021-02-04 | Esteve Pharmaceuticals, S.A. | Use of (r)-9-(2,5-difluorophenethyl)-4-ethyl-2-methyl-1-oxa-4,9-diazaspiro[5.5]undecan-3-one for the treatment of nociceptive pain, neuropathic pain, osteoarthritis pain and cancer pain, while having reduced side effects compared to opioids |
| WO2024105225A1 (en) | 2022-11-18 | 2024-05-23 | Universitat De Barcelona | Synergistic combinations of a sigma receptor 1 (s1r) antagonist and a soluble epoxide hydrolase inhibitor (sehi) and their use in the treatment of pain |
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| FR2133610B1 (cg-RX-API-DMAC7.html) * | 1971-04-15 | 1975-10-31 | Sumitomo Chemical Co | |
| US4332804A (en) * | 1981-03-23 | 1982-06-01 | Syntex (U.S.A.) Inc. | 9-[2-(3-Indolyl)ethyl]-1oxa-4,9-diazaspiro[5.5]undecan-3-ones |
| US4353900A (en) * | 1981-10-19 | 1982-10-12 | Syntex (U.S.A.) Inc. | 9-(Arylalkyl or aroylalkyl)-1-oxa-4,9-diazaspiro(5.5)undecan-3-ones |
| US6114541A (en) | 1997-03-10 | 2000-09-05 | Hoffmann-La Roche Inc. | Method for the preparation of α-Bromo-Lactam derivatives |
| RU2477136C2 (ru) * | 2004-03-03 | 2013-03-10 | Вайтал Хэлф Сайнсис Пти Лтд | Алкалоидные составы |
| DE102005030051A1 (de) | 2005-06-27 | 2006-12-28 | Grünenthal GmbH | Substituierte 1-Oxa-3,8-diazaspiro[4,5]-decan-2-on-Verbindungen und deren Verwendung zur Herstellung von Arzneimitteln |
| DE102005030061A1 (de) | 2005-06-27 | 2006-12-28 | Behr Gmbh & Co. Kg | Klimagerät |
| PT1961744E (pt) | 2005-11-18 | 2013-05-15 | Ono Pharmaceutical Co | Composto que contém um grupo básico e sua utilização |
| CN101622241B (zh) | 2007-03-01 | 2013-05-22 | 田边三菱制药株式会社 | 苯并咪唑化合物及其医药用途 |
| EP1982714A1 (en) | 2007-04-16 | 2008-10-22 | Laboratorios del Dr. Esteve S.A. | Pyrano-pyrazole-amines |
| EP2020414A1 (en) | 2007-06-20 | 2009-02-04 | Laboratorios del Dr. Esteve S.A. | spiro[piperidine-4,4'-thieno[3,2-c]pyran] derivatives and related compounds as inhibitors of the sigma receptor for the treatment of psychosis |
| EP2197876A1 (en) | 2007-08-29 | 2010-06-23 | Glaxosmithkline LLC | Thiazole and oxazole kinase inhibitors |
| CN102083839B (zh) | 2008-02-06 | 2014-03-26 | 阿斯利康(瑞典)有限公司 | 化合物 |
| US8828996B2 (en) * | 2011-03-14 | 2014-09-09 | Vertex Pharmaceuticals Incorporated | Morpholine-spirocyclic piperidine amides as modulators of ion channels |
| GB201107985D0 (en) | 2011-05-13 | 2011-06-29 | Astrazeneca Ab | Process |
| US9751881B2 (en) | 2013-07-31 | 2017-09-05 | Merck Sharp & Dohme Corp. | Inhibitors of the renal outer medullary potassium channel |
| TW201615643A (zh) | 2014-06-02 | 2016-05-01 | 伊史帝夫博士實驗室股份有限公司 | 具有多重模式抗疼痛活性之１－氧雜－４，９－二氮雜螺十一烷化合物之烷基與芳基衍生物 |
| TW201615642A (zh) | 2014-06-02 | 2016-05-01 | 伊史帝夫博士實驗室股份有限公司 | 具有多重模式抗疼痛活性的１－氧雜－４，９－二氮雜螺十一烷化合物之醯胺衍生物 |
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- 2015-06-02 MX MX2016015760A patent/MX2016015760A/es unknown
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- 2015-06-02 AU AU2015271248A patent/AU2015271248B2/en not_active Ceased
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- 2015-06-02 CA CA2949573A patent/CA2949573C/en active Active
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- 2015-06-02 WO PCT/EP2015/001115 patent/WO2015185209A1/en not_active Ceased
- 2015-06-02 MY MYPI2016704255A patent/MY177365A/en unknown
- 2015-06-02 UA UAA201613478A patent/UA124049C2/uk unknown
- 2015-06-02 KR KR1020167036612A patent/KR102468874B1/ko active Active
- 2015-06-02 AR ARP150101746A patent/AR100715A1/es active IP Right Grant
- 2015-06-02 EP EP15725236.2A patent/EP3149006B1/en active Active
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