JP6611736B2 - 疼痛に対する多様な活性を有する1−オキサ−4,9−ジアザスピロウンデカン化合物のアルキル誘導体 - Google Patents
疼痛に対する多様な活性を有する1−オキサ−4,9−ジアザスピロウンデカン化合物のアルキル誘導体 Download PDFInfo
- Publication number
- JP6611736B2 JP6611736B2 JP2016570805A JP2016570805A JP6611736B2 JP 6611736 B2 JP6611736 B2 JP 6611736B2 JP 2016570805 A JP2016570805 A JP 2016570805A JP 2016570805 A JP2016570805 A JP 2016570805A JP 6611736 B2 JP6611736 B2 JP 6611736B2
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- Japan
- Prior art keywords
- unsubstituted
- oxa
- ethyl
- substituted
- alkyl
- Prior art date
- Legal status (The legal status 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 status listed.)
- Expired - Fee Related
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- 0 CCC1OC2(CCN(CCc3ccc(C*(C)C)cc3)CC2)CN(C)C1=O Chemical compound CCC1OC2(CCN(CCc3ccc(C*(C)C)cc3)CC2)CN(C)C1=O 0.000 description 5
- FLTWQPPIRZCEEN-UHFFFAOYSA-N CC(C)C1OC2(CCN(CCc3ccccc3)CC2)CN(C)C1=O Chemical compound CC(C)C1OC2(CCN(CCc3ccccc3)CC2)CN(C)C1=O FLTWQPPIRZCEEN-UHFFFAOYSA-N 0.000 description 2
- QEHPEXFTPOUOLB-UHFFFAOYSA-N CC1OC2(CCN(CCc3ccccc3)CC2)CN(C)C1=O Chemical compound CC1OC2(CCN(CCc3ccccc3)CC2)CN(C)C1=O QEHPEXFTPOUOLB-UHFFFAOYSA-N 0.000 description 2
- QKSGTKTUVCNJNZ-UHFFFAOYSA-N CCC1OC2(CCN(CCc3ccccc3)CC2)CN(C)C1=O Chemical compound CCC1OC2(CCN(CCc3ccccc3)CC2)CN(C)C1=O QKSGTKTUVCNJNZ-UHFFFAOYSA-N 0.000 description 1
- XKPKGIFWPLKLAE-UHFFFAOYSA-N CCCCCN(CCCOC1(CC1)C(NCc(cc1)ccc1OC)=O)C(OC(C)(C)C)=O Chemical compound CCCCCN(CCCOC1(CC1)C(NCc(cc1)ccc1OC)=O)C(OC(C)(C)C)=O XKPKGIFWPLKLAE-UHFFFAOYSA-N 0.000 description 1
- KBVQQPJXAOFGJK-UHFFFAOYSA-N CCN(CC1(CCN(CCc2c[s]c(NC)n2)CC1)OC12CC1)C2=O Chemical compound CCN(CC1(CCN(CCc2c[s]c(NC)n2)CC1)OC12CC1)C2=O KBVQQPJXAOFGJK-UHFFFAOYSA-N 0.000 description 1
- VGMYQAOLKYSJON-UHFFFAOYSA-N CCN(CC1(CCN(CCc2ccccc2)CC1)OC12CC1)C2=O Chemical compound CCN(CC1(CCN(CCc2ccccc2)CC1)OC12CC1)C2=O VGMYQAOLKYSJON-UHFFFAOYSA-N 0.000 description 1
- NASMRBRQNLMHLZ-UHFFFAOYSA-N CCN(CC1(CCN(CCc2ccccc2)CC1)OC1C)C1=O Chemical compound CCN(CC1(CCN(CCc2ccccc2)CC1)OC1C)C1=O NASMRBRQNLMHLZ-UHFFFAOYSA-N 0.000 description 1
- XWIUGMQNNXVMSF-LLVKDONJSA-N C[C@H]1OC(CC2)(CCN2C(OC(C)(C)C)=O)CN(C)C1=O Chemical compound C[C@H]1OC(CC2)(CCN2C(OC(C)(C)C)=O)CN(C)C1=O XWIUGMQNNXVMSF-LLVKDONJSA-N 0.000 description 1
Classifications
-
- 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)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP14382209 | 2014-06-02 | ||
| EP14382209.6 | 2014-06-02 | ||
| PCT/EP2015/001115 WO2015185209A1 (en) | 2014-06-02 | 2015-06-02 | Alkyl derivatives of 1-oxa-4,9-diazaspiro undecane compounds having multimodal activity against pain |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2017516818A JP2017516818A (ja) | 2017-06-22 |
| JP6611736B2 true JP6611736B2 (ja) | 2019-11-27 |
Family
ID=50972618
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016570805A Expired - Fee Related JP6611736B2 (ja) | 2014-06-02 | 2015-06-02 | 疼痛に対する多様な活性を有する1−オキサ−4,9−ジアザスピロウンデカン化合物のアルキル誘導体 |
Country Status (21)
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
-
2015
- 2015-06-01 TW TW104117583A patent/TWI685497B/zh not_active IP Right Cessation
- 2015-06-02 MX MX2016015760A patent/MX2016015760A/es unknown
- 2015-06-02 CN CN201580029239.4A patent/CN106414457B/zh not_active Expired - Fee Related
- 2015-06-02 TN TN2016000509A patent/TN2016000509A1/en unknown
- 2015-06-02 SG SG10201810660QA patent/SG10201810660QA/en unknown
- 2015-06-02 AU AU2015271248A patent/AU2015271248B2/en not_active Ceased
- 2015-06-02 SG SG11201609632UA patent/SG11201609632UA/en unknown
- 2015-06-02 NZ NZ726476A patent/NZ726476A/en not_active IP Right Cessation
- 2015-06-02 CA CA2949573A patent/CA2949573C/en active Active
- 2015-06-02 RU RU2016150518A patent/RU2720406C2/ru active
- 2015-06-02 JP JP2016570805A patent/JP6611736B2/ja not_active Expired - Fee Related
- 2015-06-02 BR BR112016027825-9A patent/BR112016027825B1/pt not_active IP Right Cessation
- 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
- 2015-06-02 US US15/315,486 patent/US10246465B2/en active Active
-
2016
- 2016-11-16 IL IL249016A patent/IL249016B/en not_active IP Right Cessation
- 2016-11-18 PH PH12016502307A patent/PH12016502307B1/en unknown
- 2016-11-22 ZA ZA2016/08079A patent/ZA201608079B/en unknown
-
2019
- 2019-02-14 US US16/275,676 patent/US20190177337A1/en not_active Abandoned
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