JP2011518811A - シグマ受容体阻害剤として有用な5−メチル−1−(ナフタレン−2−イル)−1h−ピラゾール - Google Patents
シグマ受容体阻害剤として有用な5−メチル−1−(ナフタレン−2−イル)−1h−ピラゾール Download PDFInfo
- Publication number
- JP2011518811A JP2011518811A JP2011505534A JP2011505534A JP2011518811A JP 2011518811 A JP2011518811 A JP 2011518811A JP 2011505534 A JP2011505534 A JP 2011505534A JP 2011505534 A JP2011505534 A JP 2011505534A JP 2011518811 A JP2011518811 A JP 2011518811A
- Authority
- JP
- Japan
- Prior art keywords
- compound
- formula
- methyl
- pyrazol
- hydroxy
- 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.)
- Pending
Links
- RIMLIVZFVNSCQZ-UHFFFAOYSA-N Cc1cc(OCCN2CCOCC2)n[n]1-c1ccc(CCC=C2)c2c1 Chemical compound Cc1cc(OCCN2CCOCC2)n[n]1-c1ccc(CCC=C2)c2c1 RIMLIVZFVNSCQZ-UHFFFAOYSA-N 0.000 description 2
- 0 C=NC1=CC(OCC*2CCOCC2)=*=C*1c1ccc(cccc2)c2c1 Chemical compound C=NC1=CC(OCC*2CCOCC2)=*=C*1c1ccc(cccc2)c2c1 0.000 description 1
- SJRJJKPEHAURKC-UHFFFAOYSA-N CN1CCOCC1 Chemical compound CN1CCOCC1 SJRJJKPEHAURKC-UHFFFAOYSA-N 0.000 description 1
- CTZQOHLZKNNODG-KPMSDPLLSA-N Cc1cc(OCCNCCO)n[n]1-c1ccc([C@H](C2)C2C=C2)c2c1 Chemical compound Cc1cc(OCCNCCO)n[n]1-c1ccc([C@H](C2)C2C=C2)c2c1 CTZQOHLZKNNODG-KPMSDPLLSA-N 0.000 description 1
- FCFGZIFCENSKAG-UUSAFJCLSA-N Cc1cc(OCC[N]2(CCOCC2)O)n[n]1-c1cc(C=CC2[C@H]3C2)c3cc1 Chemical compound Cc1cc(OCC[N]2(CCOCC2)O)n[n]1-c1cc(C=CC2[C@H]3C2)c3cc1 FCFGZIFCENSKAG-UUSAFJCLSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D231/18—One oxygen or sulfur atom
- C07D231/20—One oxygen atom attached in position 3 or 5
- C07D231/22—One oxygen atom attached in position 3 or 5 with aryl radicals attached to ring nitrogen atoms
-
- 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
-
- 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]
-
- 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)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pain & Pain Management (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP08384005A EP2113501A1 (en) | 2008-04-25 | 2008-04-25 | 5-Methyl-1-(naphthalen-2-YL)-1H-Pyrazoles useful as sigma receptor inhibitors |
| EP08384005.8 | 2008-04-25 | ||
| PCT/EP2009/055065 WO2009130331A1 (en) | 2008-04-25 | 2009-04-27 | 5-methyl-1-(naphthalen-2-yl)-1h-pyrazoles useful as sigma receptor inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2011518811A true JP2011518811A (ja) | 2011-06-30 |
| JP2011518811A5 JP2011518811A5 (enExample) | 2012-06-07 |
Family
ID=39739580
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011505534A Pending JP2011518811A (ja) | 2008-04-25 | 2009-04-27 | シグマ受容体阻害剤として有用な5−メチル−1−(ナフタレン−2−イル)−1h−ピラゾール |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US8492425B2 (enExample) |
| EP (2) | EP2113501A1 (enExample) |
| JP (1) | JP2011518811A (enExample) |
| KR (1) | KR20110006697A (enExample) |
| CN (1) | CN102066333A (enExample) |
| AU (1) | AU2009239906A1 (enExample) |
| BR (1) | BRPI0910679A2 (enExample) |
| CA (1) | CA2722256A1 (enExample) |
| MX (1) | MX2010011674A (enExample) |
| RU (1) | RU2010147918A (enExample) |
| WO (1) | WO2009130331A1 (enExample) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2116539A1 (en) | 2008-04-25 | 2009-11-11 | Laboratorios Del. Dr. Esteve, S.A. | 1-aryl-3-aminoalkoxy-pyrazoles as sigma ligands enhancing analgesic effects of opioids and attenuating the dependency thereof |
| HRP20161128T1 (hr) * | 2009-11-25 | 2016-11-18 | Laboratorios Del Dr. Esteve, S.A. | Hidrokloridna sol 4-[2-[[5-metil-1-(2-naftalenil)-1h-pirazol-3-il]oksi]etil]morfolina |
| EP2361904A1 (en) * | 2010-02-04 | 2011-08-31 | Laboratorios Del. Dr. Esteve, S.A. | 4-[-2-[[5-methyl-1-(2-naphtalenyl)-1h-pyrazol-3-yl]oxy]ethyl]morpholine hydrochloride and crystalline forms thereof |
| EP2353598A1 (en) | 2010-02-04 | 2011-08-10 | Laboratorios Del. Dr. Esteve, S.A. | Sigma ligands for use in the prevention and/or treatment of postoperative pain |
| EP2353591A1 (en) | 2010-02-04 | 2011-08-10 | Laboratorios Del. Dr. Esteve, S.A. | Sigma ligands for potentiating the analgesic effect of opioids and opiates in post-operative pain and attenuating the dependency thereof |
| PL2531177T3 (pl) * | 2010-02-04 | 2016-11-30 | Chlorowodorek 4-[2-[[5-metylo-1-(2-naftalenylo)-1h-pirazol-3-ilo]oksy]etylo]morfoliny i solwaty | |
| EP2388005A1 (en) | 2010-05-21 | 2011-11-23 | Laboratorios Del. Dr. Esteve, S.A. | Sigma ligands for the prevention and/or treatment of emesis induced by chemotherapy or radiotherapy |
| EP2395003A1 (en) | 2010-05-27 | 2011-12-14 | Laboratorios Del. Dr. Esteve, S.A. | Pyrazole compounds as sigma receptor inhibitors |
| EP2418192A1 (en) * | 2010-07-30 | 2012-02-15 | Esteve Química, S.A. | Intermediates for the preparation of 1-aryl-pyrazol-3-one compounds useful as sigma receptors inhibitors |
| EP2415471A1 (en) | 2010-08-03 | 2012-02-08 | Laboratorios Del. Dr. Esteve, S.A. | Use of sigma ligands in opioid-induced hyperalgesia |
| EP2426111A1 (en) * | 2010-08-09 | 2012-03-07 | Laboratorios Del. Dr. Esteve, S.A. | 4-[-2-[[5-methyl-1-(2-naphtalenyl)-1h-pyrazol-3-yl]oxy]ethyl]morpholine hydrochloride amorphous solid forms |
| EP2460804A1 (en) * | 2010-12-03 | 2012-06-06 | Laboratorios Del Dr. Esteve, S.A. | 5-methyl-1-(naphthalen-2-yl)-1h-pyrazole derivatives and their use in potentiating the effect of opioid analgesics |
| EP2460519A1 (en) | 2010-12-03 | 2012-06-06 | Laboratorios Del. Dr. Esteve, S.A. | Use of sigma ligands in bone cancer pain |
| EP2524694A1 (en) | 2011-05-19 | 2012-11-21 | Laboratorios Del. Dr. Esteve, S.A. | Use of sigma ligands in diabetes type-2 associated pain |
| EP2818166A1 (en) * | 2013-06-26 | 2014-12-31 | Laboratorios del Dr. Esteve S.A. | Use of sigma receptor ligands for the prevention and treatment of pain associated to interstitial cystitis/bladder pain syndrome (IC/BPS) |
| SG11201604480PA (en) | 2013-12-17 | 2016-07-28 | Esteve Labor Dr | SEROTONIN-NOREPINEPHRINE REUPTAKE INHIBITORS (SNRIs) AND SIGMA RECEPTOR LIGANDS COMBINATIONS |
| JP6654633B2 (ja) | 2014-08-01 | 2020-02-26 | スマート ビリヤード ライティング エルエルシー | ビリヤードテーブル照明及びゲームプレイモニタ |
| MA41177A (fr) * | 2014-12-15 | 2017-10-24 | Esteve Labor Dr | Utilisation de ligands des récepteurs sigma dans l'arthrose |
| EP4475970A4 (en) | 2022-02-09 | 2025-05-14 | Martin, Blake Robert | Interactive led system for enhancing billiard gameplay |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2007098953A1 (en) * | 2006-03-01 | 2007-09-07 | Laboratorios Del Dr. Esteve, S.A. | Pyrazole derivatives as sigma receptor inhibitors |
| JP2008510767A (ja) * | 2004-08-27 | 2008-04-10 | ラボラトリオス デル ドクトール エステベ エセ.ア. | シグマ受容体阻害剤 |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9824310D0 (en) | 1998-11-05 | 1998-12-30 | Univ London | Activators of soluble guanylate cyclase |
| EP1634872A1 (en) * | 2004-08-27 | 2006-03-15 | Laboratorios Del Dr. Esteve, S.A. | Pyrazole derivatives as sigma receptor inhibitors |
| EP1829875A1 (en) * | 2006-03-01 | 2007-09-05 | Laboratorios Del Dr. Esteve, S.A. | Pyrazole derivatives as sigma receptor inhibitors |
-
2008
- 2008-04-25 EP EP08384005A patent/EP2113501A1/en not_active Withdrawn
-
2009
- 2009-04-27 KR KR1020107026489A patent/KR20110006697A/ko not_active Withdrawn
- 2009-04-27 MX MX2010011674A patent/MX2010011674A/es unknown
- 2009-04-27 AU AU2009239906A patent/AU2009239906A1/en not_active Abandoned
- 2009-04-27 US US12/988,929 patent/US8492425B2/en not_active Expired - Fee Related
- 2009-04-27 EP EP09734847A patent/EP2285781A1/en not_active Withdrawn
- 2009-04-27 BR BRPI0910679A patent/BRPI0910679A2/pt not_active IP Right Cessation
- 2009-04-27 JP JP2011505534A patent/JP2011518811A/ja active Pending
- 2009-04-27 RU RU2010147918/04A patent/RU2010147918A/ru not_active Application Discontinuation
- 2009-04-27 CN CN200980122589XA patent/CN102066333A/zh active Pending
- 2009-04-27 CA CA2722256A patent/CA2722256A1/en not_active Abandoned
- 2009-04-27 WO PCT/EP2009/055065 patent/WO2009130331A1/en not_active Ceased
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2008510767A (ja) * | 2004-08-27 | 2008-04-10 | ラボラトリオス デル ドクトール エステベ エセ.ア. | シグマ受容体阻害剤 |
| WO2007098953A1 (en) * | 2006-03-01 | 2007-09-07 | Laboratorios Del Dr. Esteve, S.A. | Pyrazole derivatives as sigma receptor inhibitors |
Also Published As
| Publication number | Publication date |
|---|---|
| EP2285781A1 (en) | 2011-02-23 |
| WO2009130331A1 (en) | 2009-10-29 |
| EP2113501A1 (en) | 2009-11-04 |
| RU2010147918A (ru) | 2012-05-27 |
| KR20110006697A (ko) | 2011-01-20 |
| CN102066333A (zh) | 2011-05-18 |
| US8492425B2 (en) | 2013-07-23 |
| MX2010011674A (es) | 2010-11-25 |
| BRPI0910679A2 (pt) | 2015-09-29 |
| US20110118253A1 (en) | 2011-05-19 |
| AU2009239906A1 (en) | 2009-10-29 |
| CA2722256A1 (en) | 2009-10-29 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20120410 |
|
| A621 | Written request for application examination |
Free format text: JAPANESE INTERMEDIATE CODE: A621 Effective date: 20120410 |
|
| A131 | Notification of reasons for refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A131 Effective date: 20131008 |
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| A02 | Decision of refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A02 Effective date: 20140304 |