ZA200308535B - 1-Oxa-3,9-diaza-spiro[5,5]undecan-2-ones derivatives and its use as antagonist of the neurikinin receptor. - Google Patents
1-Oxa-3,9-diaza-spiro[5,5]undecan-2-ones derivatives and its use as antagonist of the neurikinin receptor. Download PDFInfo
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- ZA200308535B ZA200308535B ZA200308535A ZA200308535A ZA200308535B ZA 200308535 B ZA200308535 B ZA 200308535B ZA 200308535 A ZA200308535 A ZA 200308535A ZA 200308535 A ZA200308535 A ZA 200308535A ZA 200308535 B ZA200308535 B ZA 200308535B
- Authority
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- South Africa
- Prior art keywords
- formula
- compound
- diaza
- spiro
- oxa
- Prior art date
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- 239000005557 antagonist Substances 0.000 title description 5
- KAXASJWZSSJLPG-UHFFFAOYSA-N 1-oxa-3,9-diazaspiro[5.5]undecan-2-one Chemical class O1C(=O)NCCC11CCNCC1 KAXASJWZSSJLPG-UHFFFAOYSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims description 106
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- 239000000203 mixture Substances 0.000 claims description 10
- -1 bromo, morpholinyl Chemical group 0.000 claims description 9
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 9
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- 229910052736 halogen Inorganic materials 0.000 claims description 9
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- FEYUTRZPSFLEST-UHFFFAOYSA-N spiro[5.5]undecan-4-one Chemical compound C1C(=O)CCCC11CCCCC1 FEYUTRZPSFLEST-UHFFFAOYSA-N 0.000 claims description 4
- ZECJUCGRCJUNIL-UHFFFAOYSA-N 9-[3,5-bis(trifluoromethyl)benzoyl]-3-(1-methylpiperidin-4-yl)-5-phenyl-1-oxa-3,9-diazaspiro[5.5]undecan-2-one Chemical compound C1CN(C)CCC1N1C(=O)OC2(CCN(CC2)C(=O)C=2C=C(C=C(C=2)C(F)(F)F)C(F)(F)F)C(C=2C=CC=CC=2)C1 ZECJUCGRCJUNIL-UHFFFAOYSA-N 0.000 claims description 3
- KOOSRSYKRYWAAS-UHFFFAOYSA-N 9-[3,5-bis(trifluoromethyl)benzoyl]-5-(3,4-dichlorophenyl)-1-oxa-3,9-diazaspiro[5.5]undecan-2-one Chemical compound FC(F)(F)C1=CC(C(F)(F)F)=CC(C(=O)N2CCC3(CC2)C(CNC(=O)O3)C=2C=C(Cl)C(Cl)=CC=2)=C1 KOOSRSYKRYWAAS-UHFFFAOYSA-N 0.000 claims description 3
- HGXVVFLYFCJJSU-UHFFFAOYSA-N 9-[3,5-bis(trifluoromethyl)benzoyl]-5-(3,4-difluorophenyl)-1-oxa-3,9-diazaspiro[5.5]undecan-2-one Chemical compound C1=C(F)C(F)=CC=C1C1C2(CCN(CC2)C(=O)C=2C=C(C=C(C=2)C(F)(F)F)C(F)(F)F)OC(=O)NC1 HGXVVFLYFCJJSU-UHFFFAOYSA-N 0.000 claims description 3
- SEAFPVXMSCTQLM-UHFFFAOYSA-N 9-[3,5-bis(trifluoromethyl)benzoyl]-5-(3-chlorophenyl)-1-oxa-3,9-diazaspiro[5.5]undecan-2-one Chemical compound FC(F)(F)C1=CC(C(F)(F)F)=CC(C(=O)N2CCC3(CC2)C(CNC(=O)O3)C=2C=C(Cl)C=CC=2)=C1 SEAFPVXMSCTQLM-UHFFFAOYSA-N 0.000 claims description 3
- 125000000623 heterocyclic group Chemical group 0.000 claims description 3
- MIGNBVWFGCBAJP-UHFFFAOYSA-N 9-[3,5-bis(trifluoromethyl)benzoyl]-3-(3-hydroxypropyl)-5-phenyl-1-oxa-3,9-diazaspiro[5.5]undecan-2-one Chemical compound C1CN(C(=O)C=2C=C(C=C(C=2)C(F)(F)F)C(F)(F)F)CCC21OC(=O)N(CCCO)CC2C1=CC=CC=C1 MIGNBVWFGCBAJP-UHFFFAOYSA-N 0.000 claims description 2
- USKRLFGVPFHMNS-UHFFFAOYSA-N 9-[3,5-bis(trifluoromethyl)benzoyl]-3-(3-morpholin-4-ylpropyl)-5-phenyl-1-oxa-3,9-diazaspiro[5.5]undecan-2-one Chemical compound FC(F)(F)C1=CC(C(F)(F)F)=CC(C(=O)N2CCC3(CC2)C(CN(CCCN2CCOCC2)C(=O)O3)C=2C=CC=CC=2)=C1 USKRLFGVPFHMNS-UHFFFAOYSA-N 0.000 claims description 2
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- 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
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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
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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
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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- A—HUMAN NECESSITIES
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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
- A61P25/24—Antidepressants
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- 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
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)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
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- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
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- Pulmonology (AREA)
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- Orthopedic Medicine & Surgery (AREA)
- Rheumatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Otolaryngology (AREA)
- Pain & Pain Management (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 (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP01111644 | 2001-05-14 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ZA200308535B true ZA200308535B (en) | 2005-01-31 |
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Family Applications (1)
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| ZA200308535A ZA200308535B (en) | 2001-05-14 | 2003-10-31 | 1-Oxa-3,9-diaza-spiro[5,5]undecan-2-ones derivatives and its use as antagonist of the neurikinin receptor. |
Country Status (17)
| Country | Link |
|---|---|
| US (1) | US6599900B2 (https=) |
| EP (1) | EP1390372B1 (https=) |
| JP (1) | JP4056887B2 (https=) |
| KR (1) | KR100618063B1 (https=) |
| CN (1) | CN1264847C (https=) |
| AR (1) | AR033631A1 (https=) |
| AT (1) | ATE401333T1 (https=) |
| AU (1) | AU2002342238B2 (https=) |
| BR (1) | BR0209604A (https=) |
| CA (1) | CA2447329C (https=) |
| DE (1) | DE60227657D1 (https=) |
| DK (1) | DK1390372T3 (https=) |
| ES (1) | ES2310206T3 (https=) |
| MX (1) | MXPA03010321A (https=) |
| PT (1) | PT1390372E (https=) |
| WO (1) | WO2002092604A1 (https=) |
| ZA (1) | ZA200308535B (https=) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2006132465A (ru) * | 2004-02-10 | 2008-03-20 | Ф.Хоффманн-Ля Рош Аг (Ch) | Модуляторы хемокинового рецептора ccr5 |
| KR20070094666A (ko) | 2005-02-25 | 2007-09-20 | 에프. 호프만-라 로슈 아게 | 약제 물질 분산성이 향상된 정제 |
| DE602006014531D1 (de) * | 2005-03-03 | 2010-07-08 | Janssen Pharmaceutica Nv | Substituierte oxadiazaspiro-ä5.5ü-undecanonderivate und ihre verwendung als neurokininantagonisten |
| NZ556628A (en) | 2005-03-08 | 2009-09-25 | Janssen Pharmaceutica Nv | Diaza-spiro-[4.4]-nonane derivatives as neurokinin (NK1) antagonists |
| US7470684B2 (en) * | 2007-01-03 | 2008-12-30 | Hoffmann-La Roche Inc. | Spiropiperidine derivatives as NK3 antagonists |
| EP2117538A1 (en) | 2007-01-24 | 2009-11-18 | Glaxo Group Limited | Pharmaceutical compositions comprising 2-methoxy-5- (5-trifluoromethyl-tetrazol-i-yl-benzyl) - (2s-phenyl-piperidin-3s-yl-) |
| WO2008119663A1 (en) | 2007-03-29 | 2008-10-09 | F. Hoffmann-La Roche Ag | Heterocyclic antiviral compounds |
| UA121775C2 (uk) | 2015-07-31 | 2020-07-27 | Пфайзер Інк. | 1,1,1-трифтор-3-гідроксипропан-2-ілкарбаматні похідні та 1,1,1-трифтор-4-гідроксибутан-2-ілкарбаматні похідні як інгібітори magl |
| EP3571191A1 (en) | 2017-01-20 | 2019-11-27 | Pfizer Inc | 1,1,1-trifluoro-3-hydroxypropan-2-yl carbamate derivatives as magl inhibitors |
| EP3571202B1 (en) | 2017-01-23 | 2021-06-30 | Pfizer Inc. | Heterocyclic spiro compounds as magl inhibitors |
| WO2020048826A1 (en) | 2018-09-03 | 2020-03-12 | Bayer Aktiengesellschaft | 5-substituted 1-oxa-3,9-diazaspiro[5.5]undecan-2-one compounds |
| WO2020048827A1 (en) | 2018-09-03 | 2020-03-12 | Bayer Aktiengesellschaft | 1, 3, 9-triazaspiro[5.5] undecan-2-one compounds |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB2131021B (en) * | 1982-11-24 | 1985-12-18 | Erba Farmitalia | Antipsychotic benzoxazines |
| IL111960A (en) * | 1993-12-17 | 1999-12-22 | Merck & Co Inc | Morpholines and thiomorpholines their preparation and pharmaceutical compositions containing them |
| WO1997011940A1 (en) * | 1995-09-29 | 1997-04-03 | Eli Lilly And Company | Spiro compounds as inhibitors of fibrinogen-dependent platelet aggregation |
-
2002
- 2002-05-06 CN CNB028094735A patent/CN1264847C/zh not_active Expired - Fee Related
- 2002-05-06 EP EP02742943A patent/EP1390372B1/en not_active Expired - Lifetime
- 2002-05-06 AT AT02742943T patent/ATE401333T1/de not_active IP Right Cessation
- 2002-05-06 KR KR1020037014713A patent/KR100618063B1/ko not_active Expired - Fee Related
- 2002-05-06 PT PT02742943T patent/PT1390372E/pt unknown
- 2002-05-06 DK DK02742943T patent/DK1390372T3/da active
- 2002-05-06 DE DE60227657T patent/DE60227657D1/de not_active Expired - Lifetime
- 2002-05-06 MX MXPA03010321A patent/MXPA03010321A/es active IP Right Grant
- 2002-05-06 ES ES02742943T patent/ES2310206T3/es not_active Expired - Lifetime
- 2002-05-06 JP JP2002589488A patent/JP4056887B2/ja not_active Expired - Fee Related
- 2002-05-06 AU AU2002342238A patent/AU2002342238B2/en not_active Ceased
- 2002-05-06 WO PCT/EP2002/004935 patent/WO2002092604A1/en not_active Ceased
- 2002-05-06 CA CA002447329A patent/CA2447329C/en not_active Expired - Fee Related
- 2002-05-06 BR BR0209604-8A patent/BR0209604A/pt not_active IP Right Cessation
- 2002-05-10 AR ARP020101705A patent/AR033631A1/es unknown
- 2002-05-10 US US10/143,431 patent/US6599900B2/en not_active Expired - Fee Related
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2003
- 2003-10-31 ZA ZA200308535A patent/ZA200308535B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| DK1390372T3 (da) | 2008-09-15 |
| EP1390372B1 (en) | 2008-07-16 |
| CA2447329C (en) | 2009-07-28 |
| KR100618063B1 (ko) | 2006-08-30 |
| MXPA03010321A (es) | 2004-02-17 |
| ES2310206T3 (es) | 2009-01-01 |
| CA2447329A1 (en) | 2002-11-21 |
| DE60227657D1 (de) | 2008-08-28 |
| AU2002342238B2 (en) | 2007-01-25 |
| CN1264847C (zh) | 2006-07-19 |
| WO2002092604A1 (en) | 2002-11-21 |
| JP2004534758A (ja) | 2004-11-18 |
| EP1390372A1 (en) | 2004-02-25 |
| US6599900B2 (en) | 2003-07-29 |
| KR20030094405A (ko) | 2003-12-11 |
| AR033631A1 (es) | 2003-12-26 |
| JP4056887B2 (ja) | 2008-03-05 |
| CN1507449A (zh) | 2004-06-23 |
| ATE401333T1 (de) | 2008-08-15 |
| PT1390372E (pt) | 2008-08-25 |
| BR0209604A (pt) | 2004-03-23 |
| US20030004163A1 (en) | 2003-01-02 |
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