AU2003215603A1 - Azaspiro compounds for the treatment of pain - Google Patents
Azaspiro compounds for the treatment of pain Download PDFInfo
- Publication number
- AU2003215603A1 AU2003215603A1 AU2003215603A AU2003215603A AU2003215603A1 AU 2003215603 A1 AU2003215603 A1 AU 2003215603A1 AU 2003215603 A AU2003215603 A AU 2003215603A AU 2003215603 A AU2003215603 A AU 2003215603A AU 2003215603 A1 AU2003215603 A1 AU 2003215603A1
- Authority
- AU
- Australia
- Prior art keywords
- azaspiro
- amino
- sulfonyl
- amido
- 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.)
- Abandoned
Links
- 150000008627 azaspiro compounds Chemical class 0.000 title claims abstract description 54
- 208000002193 Pain Diseases 0.000 title claims abstract description 27
- 239000003814 drug Substances 0.000 claims abstract description 26
- 150000003839 salts Chemical class 0.000 claims abstract description 14
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 13
- 239000000546 pharmaceutical excipient Substances 0.000 claims abstract description 6
- -1 2-azaspiro[4.5]decane-3-thion 2-azaspiro[4.4]nonane-3-thion 2-azaspiro[4.6]undecane-3-thion Chemical compound 0.000 claims description 56
- 229940079593 drug Drugs 0.000 claims description 22
- 208000004296 neuralgia Diseases 0.000 claims description 20
- 208000021722 neuropathic pain Diseases 0.000 claims description 20
- 150000001875 compounds Chemical class 0.000 claims description 19
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- 238000002483 medication Methods 0.000 claims description 6
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- 125000000217 alkyl group Chemical group 0.000 abstract description 49
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract description 30
- 125000003368 amide group Chemical group 0.000 abstract description 28
- 238000012360 testing method Methods 0.000 abstract description 24
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- 235000006408 oxalic acid Nutrition 0.000 description 1
- 230000007310 pathophysiology Effects 0.000 description 1
- 125000003538 pentan-3-yl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])C([H])([H])[H] 0.000 description 1
- 125000001147 pentyl group Chemical group C(CCCC)* 0.000 description 1
- 230000002093 peripheral effect Effects 0.000 description 1
- 210000001428 peripheral nervous system Anatomy 0.000 description 1
- 239000000825 pharmaceutical preparation Substances 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 238000001556 precipitation Methods 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- 238000011552 rat model Methods 0.000 description 1
- 239000011541 reaction mixture Substances 0.000 description 1
- 230000003134 recirculating effect Effects 0.000 description 1
- 239000012266 salt solution Substances 0.000 description 1
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 1
- 125000003548 sec-pentyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 1
- 230000036280 sedation Effects 0.000 description 1
- 239000000932 sedative agent Substances 0.000 description 1
- 230000001624 sedative effect Effects 0.000 description 1
- 238000000926 separation method Methods 0.000 description 1
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 description 1
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 description 1
- 238000001228 spectrum Methods 0.000 description 1
- 210000000278 spinal cord Anatomy 0.000 description 1
- 239000007921 spray Substances 0.000 description 1
- 239000003381 stabilizer Substances 0.000 description 1
- 238000007920 subcutaneous administration Methods 0.000 description 1
- 239000001384 succinic acid Substances 0.000 description 1
- 235000011044 succinic acid Nutrition 0.000 description 1
- BDHFUVZGWQCTTF-UHFFFAOYSA-M sulfonate Chemical compound [O-]S(=O)=O BDHFUVZGWQCTTF-UHFFFAOYSA-M 0.000 description 1
- 239000000829 suppository Substances 0.000 description 1
- 230000007428 synaptic transmission, GABAergic Effects 0.000 description 1
- 230000007593 synaptic transmission, glutaminergic Effects 0.000 description 1
- 239000003826 tablet Substances 0.000 description 1
- 239000011975 tartaric acid Substances 0.000 description 1
- 235000002906 tartaric acid Nutrition 0.000 description 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 125000001973 tert-pentyl group Chemical group [H]C([H])([H])C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 231100000816 toxic dose Toxicity 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 1
- RSJKGSCJYJTIGS-UHFFFAOYSA-N undecane Chemical class CCCCCCCCCCC RSJKGSCJYJTIGS-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/54—Spiro-condensed
-
- 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
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/10—Spiro-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D497/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having oxygen and sulfur atoms as the only ring hetero atoms
- C07D497/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having oxygen and sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D497/10—Spiro-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pain & Pain Management (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Engineering & Computer Science (AREA)
- Biomedical Technology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Indole Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE10210190A DE10210190A1 (de) | 2002-03-07 | 2002-03-07 | Aza-Spiroverbindungen |
| DE10210190.6 | 2002-03-07 | ||
| PCT/EP2003/001986 WO2003074486A1 (de) | 2002-03-07 | 2003-02-27 | Aza-spiroverbindungen zur behandlug von schmerzen |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| AU2003215603A1 true AU2003215603A1 (en) | 2003-09-16 |
| AU2003215603A2 AU2003215603A2 (en) | 2003-09-16 |
Family
ID=27771112
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2003215603A Abandoned AU2003215603A1 (en) | 2002-03-07 | 2003-02-27 | Azaspiro compounds for the treatment of pain |
Country Status (19)
| Country | Link |
|---|---|
| US (1) | US20050288351A1 (enExample) |
| EP (2) | EP1520854A3 (enExample) |
| JP (1) | JP2005526745A (enExample) |
| KR (1) | KR20040091638A (enExample) |
| CN (1) | CN1324011C (enExample) |
| AT (1) | ATE298745T1 (enExample) |
| AU (1) | AU2003215603A1 (enExample) |
| BR (1) | BR0307922A (enExample) |
| CA (1) | CA2477124A1 (enExample) |
| DE (2) | DE10210190A1 (enExample) |
| ES (1) | ES2242944T3 (enExample) |
| MX (1) | MXPA04008669A (enExample) |
| NO (1) | NO20044239L (enExample) |
| PL (1) | PL372431A1 (enExample) |
| PT (1) | PT1485352E (enExample) |
| RU (1) | RU2322438C2 (enExample) |
| UA (1) | UA78987C2 (enExample) |
| WO (1) | WO2003074486A1 (enExample) |
| ZA (1) | ZA200406245B (enExample) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW201607923A (zh) * | 2014-07-15 | 2016-03-01 | 歌林達有限公司 | 被取代之氮螺環（４．５）癸烷衍生物 |
| CN107216335B (zh) * | 2017-06-29 | 2019-04-30 | 上海药明康德新药开发有限公司 | 一种叔丁基1-(羟甲基)-3-氧杂-9-氮杂螺[5.5]十一烷-9-甲酸基酯制法 |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2866734A (en) * | 1956-12-05 | 1958-12-30 | Us Vitamin Corp | 3-pyridylethyl 2, 4-oxazolidinediones and process |
| US3150143A (en) * | 1960-07-19 | 1964-09-22 | Geschicketer Fund For Medical | Therapeutically active nu-substituted azaspiranes |
| US3398151A (en) * | 1966-02-01 | 1968-08-20 | Mead Johnson & Co | Azaspirodecanediones and azaspiroundecanediones |
| US3629276A (en) * | 1969-07-16 | 1971-12-21 | Abbott Lab | 2-amino-5-spiro-substituted-oxazo compounds |
| US4430335A (en) * | 1983-02-09 | 1984-02-07 | Hoechst-Roussel Pharmaceuticals Inc. | Substituted 1-azaspiro[4,5]decanes and their analgesic compositions |
| GB8916447D0 (en) * | 1989-07-19 | 1989-09-06 | Ici Plc | Composition,process and use |
| US5132451A (en) * | 1989-08-25 | 1992-07-21 | Warner-Lambert Company | Process for cyclic amino acid anticonvulsant compounds |
| US5319135A (en) * | 1989-08-25 | 1994-06-07 | Warner-Lambert Company | Process for cyclic amino acid anticonvulsant compounds |
| RU95114363A (ru) * | 1992-11-09 | 1997-03-20 | Дзе Бутс Компани ПЛС. (GB) | Производные азаспиросоединений, способ их получения, фармацевтическая композиция, средства для лечения ожирения, средства для лечения аффективных расстройств |
| US5925672A (en) * | 1996-12-06 | 1999-07-20 | Neurosciences Research Foundation, Inc. | Methods of treating mental diseases, inflammation and pain |
| GB9708484D0 (en) * | 1997-04-25 | 1997-06-18 | Merck Sharp & Dohme | Therapeutic agents |
| DE19732928C2 (de) * | 1997-07-31 | 2000-05-18 | Gruenenthal Gmbh | Verwendung substituierter Imidazolidin-2,4-dion-Verbindungen als Schmerzmittel |
| US5948807A (en) * | 1997-09-03 | 1999-09-07 | Regents Of The University Of Minnesota | Spiroindanamines and Spiroindanimides |
| DE19751062A1 (de) * | 1997-11-18 | 1999-07-08 | Univ Ludwigs Albert | An 4-Stellung substituierte 2-Pyrrolidinon-Derivate zur Verringerung des extrazellulären Glutamat-Spiegels |
| JP2002516312A (ja) * | 1998-05-26 | 2002-06-04 | ワーナー−ランバート・カンパニー | カルシウムチャンネルのα２δサブユニットに対する親和性を有する立体配座的に制約されたアミノ酸化合物 |
-
2002
- 2002-03-07 DE DE10210190A patent/DE10210190A1/de not_active Ceased
-
2003
- 2003-02-27 AT AT03743342T patent/ATE298745T1/de not_active IP Right Cessation
- 2003-02-27 EP EP04029311A patent/EP1520854A3/de not_active Withdrawn
- 2003-02-27 KR KR10-2004-7012680A patent/KR20040091638A/ko not_active Ceased
- 2003-02-27 MX MXPA04008669A patent/MXPA04008669A/es not_active Application Discontinuation
- 2003-02-27 CN CNB038054388A patent/CN1324011C/zh not_active Expired - Fee Related
- 2003-02-27 UA UA20041008091A patent/UA78987C2/uk unknown
- 2003-02-27 EP EP03743342A patent/EP1485352B1/de not_active Expired - Lifetime
- 2003-02-27 CA CA002477124A patent/CA2477124A1/en not_active Abandoned
- 2003-02-27 AU AU2003215603A patent/AU2003215603A1/en not_active Abandoned
- 2003-02-27 RU RU2004129769/04A patent/RU2322438C2/ru not_active IP Right Cessation
- 2003-02-27 BR BR0307922-8A patent/BR0307922A/pt not_active IP Right Cessation
- 2003-02-27 JP JP2003572956A patent/JP2005526745A/ja active Pending
- 2003-02-27 DE DE50300710T patent/DE50300710D1/de not_active Expired - Fee Related
- 2003-02-27 ES ES03743342T patent/ES2242944T3/es not_active Expired - Lifetime
- 2003-02-27 WO PCT/EP2003/001986 patent/WO2003074486A1/de not_active Ceased
- 2003-02-27 PT PT03743342T patent/PT1485352E/pt unknown
- 2003-02-27 PL PL03372431A patent/PL372431A1/xx not_active Application Discontinuation
-
2004
- 2004-08-05 ZA ZA200406245A patent/ZA200406245B/xx unknown
- 2004-09-07 US US10/936,134 patent/US20050288351A1/en not_active Abandoned
- 2004-10-06 NO NO20044239A patent/NO20044239L/no not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| MXPA04008669A (es) | 2004-12-06 |
| EP1520854A3 (de) | 2007-02-21 |
| CN1324011C (zh) | 2007-07-04 |
| KR20040091638A (ko) | 2004-10-28 |
| CN1639122A (zh) | 2005-07-13 |
| DE50300710D1 (de) | 2005-08-04 |
| DE10210190A1 (de) | 2003-09-25 |
| BR0307922A (pt) | 2004-12-21 |
| CA2477124A1 (en) | 2003-09-12 |
| EP1520854A2 (de) | 2005-04-06 |
| EP1485352A1 (de) | 2004-12-15 |
| WO2003074486A1 (de) | 2003-09-12 |
| UA78987C2 (en) | 2007-05-10 |
| HK1080468A1 (zh) | 2006-04-28 |
| RU2004129769A (ru) | 2005-07-10 |
| ATE298745T1 (de) | 2005-07-15 |
| PT1485352E (pt) | 2005-10-31 |
| US20050288351A1 (en) | 2005-12-29 |
| ES2242944T3 (es) | 2005-11-16 |
| JP2005526745A (ja) | 2005-09-08 |
| NO20044239L (no) | 2004-12-01 |
| ZA200406245B (en) | 2005-06-13 |
| PL372431A1 (en) | 2005-07-25 |
| RU2322438C2 (ru) | 2008-04-20 |
| EP1485352B1 (de) | 2005-06-29 |
| AU2003215603A2 (en) | 2003-09-16 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| DA3 | Amendments made section 104 |
Free format text: THE NATURE OF THE AMENDMENT IS AS SHOWN IN THE STATEMENT(S) FILED 10 SEP 2004 |
|
| MK4 | Application lapsed section 142(2)(d) - no continuation fee paid for the application |