JP2009528318A5 - - Google Patents
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- JP2009528318A5 JP2009528318A5 JP2008556726A JP2008556726A JP2009528318A5 JP 2009528318 A5 JP2009528318 A5 JP 2009528318A5 JP 2008556726 A JP2008556726 A JP 2008556726A JP 2008556726 A JP2008556726 A JP 2008556726A JP 2009528318 A5 JP2009528318 A5 JP 2009528318A5
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- JP
- Japan
- Prior art keywords
- group
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- monosubstituted
- branched
- unbranched
- 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.)
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- 125000001424 substituent group Chemical group 0.000 claims 37
- 150000001875 compounds Chemical class 0.000 claims 23
- 125000005842 heteroatom Chemical group 0.000 claims 16
- 125000002950 monocyclic group Chemical group 0.000 claims 16
- 125000003367 polycyclic group Chemical group 0.000 claims 15
- 125000000753 cycloalkyl group Chemical group 0.000 claims 14
- 229920006395 saturated elastomer Polymers 0.000 claims 14
- 125000001072 heteroaryl group Chemical group 0.000 claims 11
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 11
- 125000002877 alkyl aryl group Chemical group 0.000 claims 10
- 125000005213 alkyl heteroaryl group Chemical group 0.000 claims 9
- 125000003118 aryl group Chemical group 0.000 claims 9
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 8
- 239000000470 constituent Substances 0.000 claims 7
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 6
- YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical group C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 claims 5
- 125000005119 alkyl cycloalkyl group Chemical group 0.000 claims 5
- 208000006575 hypertriglyceridemia Diseases 0.000 claims 5
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 5
- RWRDLPDLKQPQOW-UHFFFAOYSA-N tetrahydropyrrole Natural products C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims 5
- 208000031226 Hyperlipidaemia Diseases 0.000 claims 4
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical group C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims 4
- 230000002159 abnormal effect Effects 0.000 claims 4
- 125000000217 alkyl group Chemical group 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 4
- 208000035475 disorder Diseases 0.000 claims 4
- 229910052757 nitrogen Inorganic materials 0.000 claims 4
- 125000004430 oxygen atom Chemical group O* 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 239000012453 solvate Substances 0.000 claims 4
- 102000004895 Lipoproteins Human genes 0.000 claims 3
- 108090001030 Lipoproteins Proteins 0.000 claims 3
- 125000001931 aliphatic group Chemical group 0.000 claims 3
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 3
- 238000006243 chemical reaction Methods 0.000 claims 3
- 125000004122 cyclic group Chemical group 0.000 claims 3
- 239000000203 mixture Substances 0.000 claims 3
- 125000001624 naphthyl group Chemical group 0.000 claims 3
- UFTFJSFQGQCHQW-UHFFFAOYSA-N triformin Chemical compound O=COCC(OC=O)COC=O UFTFJSFQGQCHQW-UHFFFAOYSA-N 0.000 claims 3
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 2
- 208000004454 Hyperalgesia Diseases 0.000 claims 2
- 208000035150 Hypercholesterolemia Diseases 0.000 claims 2
- 208000002193 Pain Diseases 0.000 claims 2
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical group C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 claims 2
- ZPUCINDJVBIVPJ-LJISPDSOSA-N cocaine Chemical compound O([C@H]1C[C@@H]2CC[C@@H](N2C)[C@H]1C(=O)OC)C(=O)C1=CC=CC=C1 ZPUCINDJVBIVPJ-LJISPDSOSA-N 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 125000000623 heterocyclic group Chemical group 0.000 claims 2
- 208000020346 hyperlipoproteinemia Diseases 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 238000002360 preparation method Methods 0.000 claims 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 2
- 238000006467 substitution reaction Methods 0.000 claims 2
- SNICXCGAKADSCV-JTQLQIEISA-N (-)-Nicotine Chemical compound CN1CCC[C@H]1C1=CC=CN=C1 SNICXCGAKADSCV-JTQLQIEISA-N 0.000 claims 1
- KWTSXDURSIMDCE-QMMMGPOBSA-N (S)-amphetamine Chemical compound C[C@H](N)CC1=CC=CC=C1 KWTSXDURSIMDCE-QMMMGPOBSA-N 0.000 claims 1
- MEPYQUAPJWBMJH-UHFFFAOYSA-N 1-[1-(3,4-dichlorophenyl)pyrazol-3-yl]oxy-3-(4-methylpiperazin-1-yl)propan-2-ol Chemical compound C1CN(C)CCN1CC(O)COC1=NN(C=2C=C(Cl)C(Cl)=CC=2)C=C1 MEPYQUAPJWBMJH-UHFFFAOYSA-N 0.000 claims 1
- NMQPZCLURQSRFP-UHFFFAOYSA-N 1-[1-(3,4-dichlorophenyl)pyrazol-3-yl]oxy-3-morpholin-4-ylpropan-2-ol Chemical compound C1COCCN1CC(O)COC(=N1)C=CN1C1=CC=C(Cl)C(Cl)=C1 NMQPZCLURQSRFP-UHFFFAOYSA-N 0.000 claims 1
- WDRXQTXIYGMMOD-UHFFFAOYSA-N 1-[1-(3,4-dichlorophenyl)pyrazol-3-yl]oxy-3-piperidin-1-ylpropan-2-ol Chemical compound C1CCCCN1CC(O)COC(=N1)C=CN1C1=CC=C(Cl)C(Cl)=C1 WDRXQTXIYGMMOD-UHFFFAOYSA-N 0.000 claims 1
- OOTHURWXYHJWGY-UHFFFAOYSA-N 1-[1-(3,4-dichlorophenyl)pyrazol-3-yl]oxy-3-pyrrolidin-1-ylpropan-2-ol Chemical compound C1CCCN1CC(O)COC(=N1)C=CN1C1=CC=C(Cl)C(Cl)=C1 OOTHURWXYHJWGY-UHFFFAOYSA-N 0.000 claims 1
- AILGBBRMXHWWAF-UHFFFAOYSA-N 1-[2-[2-[1-(3,4-dichlorophenyl)pyrazol-3-yl]oxyethoxy]ethyl]piperidine Chemical compound C1=C(Cl)C(Cl)=CC=C1N1N=C(OCCOCCN2CCCCC2)C=C1 AILGBBRMXHWWAF-UHFFFAOYSA-N 0.000 claims 1
- -1 2- (1- (3,4-dichlorophenyl) -1H-pyrazol-3-yloxy) ethyl Chemical group 0.000 claims 1
- 125000000094 2-phenylethyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])C([H])([H])* 0.000 claims 1
- PUBTUBYIGOZPBV-UHFFFAOYSA-N 4-[2-[2-[1-(3,4-dichlorophenyl)pyrazol-3-yl]oxyethoxy]ethyl]morpholine Chemical compound C1=C(Cl)C(Cl)=CC=C1N1N=C(OCCOCCN2CCOCC2)C=C1 PUBTUBYIGOZPBV-UHFFFAOYSA-N 0.000 claims 1
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims 1
- 208000019901 Anxiety disease Diseases 0.000 claims 1
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- 208000028698 Cognitive impairment Diseases 0.000 claims 1
- 208000016192 Demyelinating disease Diseases 0.000 claims 1
- 206010012735 Diarrhoea Diseases 0.000 claims 1
- 208000012661 Dyskinesia Diseases 0.000 claims 1
- 208000035154 Hyperesthesia Diseases 0.000 claims 1
- 206010020772 Hypertension Diseases 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 206010065390 Inflammatory pain Diseases 0.000 claims 1
- 208000032382 Ischaemic stroke Diseases 0.000 claims 1
- 208000020358 Learning disease Diseases 0.000 claims 1
- 208000019695 Migraine disease Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 206010040047 Sepsis Diseases 0.000 claims 1
- 208000006011 Stroke Diseases 0.000 claims 1
- 206010060755 Type V hyperlipidaemia Diseases 0.000 claims 1
- 208000025865 Ulcer Diseases 0.000 claims 1
- 125000002015 acyclic group Chemical group 0.000 claims 1
- 206010053552 allodynia Diseases 0.000 claims 1
- 150000001412 amines Chemical class 0.000 claims 1
- 229940025084 amphetamine Drugs 0.000 claims 1
- 230000036506 anxiety Effects 0.000 claims 1
- 230000006793 arrhythmia Effects 0.000 claims 1
- 206010003119 arrhythmia Diseases 0.000 claims 1
- 206010003246 arthritis Diseases 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 229960003920 cocaine Drugs 0.000 claims 1
- 208000010877 cognitive disease Diseases 0.000 claims 1
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 206010013663 drug dependence Diseases 0.000 claims 1
- 206010015037 epilepsy Diseases 0.000 claims 1
- 229960004756 ethanol Drugs 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 230000036541 health Effects 0.000 claims 1
- 125000004404 heteroalkyl group Chemical group 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 201000003723 learning disability Diseases 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 206010027599 migraine Diseases 0.000 claims 1
- 125000004108 n-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
- 208000004296 neuralgia Diseases 0.000 claims 1
- 230000004770 neurodegeneration Effects 0.000 claims 1
- 208000015122 neurodegenerative disease Diseases 0.000 claims 1
- 208000021722 neuropathic pain Diseases 0.000 claims 1
- 229960002715 nicotine Drugs 0.000 claims 1
- SNICXCGAKADSCV-UHFFFAOYSA-N nicotine Natural products CN1CCCC1C1=CC=CN=C1 SNICXCGAKADSCV-UHFFFAOYSA-N 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 125000004193 piperazinyl group Chemical group 0.000 claims 1
- 125000003386 piperidinyl group Chemical group 0.000 claims 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 201000000980 schizophrenia Diseases 0.000 claims 1
- 208000013223 septicemia Diseases 0.000 claims 1
- 108010085082 sigma receptors Proteins 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
- 231100000397 ulcer Toxicity 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP06004288A EP1829873A1 (en) | 2006-03-02 | 2006-03-02 | Pyrrazole derivatives as sigma receptors antagonists |
| PCT/EP2007/001827 WO2007098964A2 (en) | 2006-03-02 | 2007-03-02 | Pyrrazole derivatives as sigma receptors antagonists |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2009528318A JP2009528318A (ja) | 2009-08-06 |
| JP2009528318A5 true JP2009528318A5 (enExample) | 2010-04-15 |
Family
ID=36440951
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2008556726A Pending JP2009528318A (ja) | 2006-03-02 | 2007-03-02 | シグマ受容体化合物 |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US8138186B2 (enExample) |
| EP (2) | EP1829873A1 (enExample) |
| JP (1) | JP2009528318A (enExample) |
| CN (1) | CN101395152B (enExample) |
| CA (1) | CA2640754A1 (enExample) |
| ES (1) | ES2572985T3 (enExample) |
| MX (1) | MX2008011019A (enExample) |
| WO (1) | WO2007098964A2 (enExample) |
Families Citing this family (11)
| 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 |
| 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 |
| 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 |
| EP2415471A1 (en) | 2010-08-03 | 2012-02-08 | Laboratorios Del. Dr. Esteve, S.A. | Use of sigma ligands in opioid-induced hyperalgesia |
| EP2524694A1 (en) | 2011-05-19 | 2012-11-21 | Laboratorios Del. Dr. Esteve, S.A. | Use of sigma ligands in diabetes type-2 associated pain |
| SG11201604480PA (en) | 2013-12-17 | 2016-07-28 | Esteve Labor Dr | SEROTONIN-NOREPINEPHRINE REUPTAKE INHIBITORS (SNRIs) AND SIGMA RECEPTOR LIGANDS COMBINATIONS |
| EP2929883A1 (en) * | 2014-04-08 | 2015-10-14 | Institut Pasteur | Pyrazole derivatives as dihydroorotate dehydrogenase (DHODH) inhibitors |
| CN104829541B (zh) * | 2015-05-05 | 2017-06-30 | 江苏豪森药业集团有限公司 | 高选择性及高纯度制备吗啉硝唑的方法 |
| US12428378B2 (en) | 2019-09-10 | 2025-09-30 | University of Pittsburgh—of the Commonwealth System of Higher Education | Methods and materials for increasing level of phosphorylated AMPK protein |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DD118636A1 (enExample) * | 1975-04-10 | 1976-03-12 | ||
| DD118637A1 (enExample) * | 1975-04-10 | 1976-03-12 | ||
| DE4341749A1 (de) * | 1993-12-08 | 1995-06-14 | Kali Chemie Pharma Gmbh | 3-(Phenylalkylaminoalkyloxy)-5-phenylpyrazol- Verbindungen sowie Verfahren und Zwischenprodukte zu ihrer Herstellung und diese Verbindungen enthaltende Arzneimittel |
| IL112764A0 (en) * | 1994-03-18 | 1995-05-26 | Ferrer Int | New chromene derivatives |
| US6514977B1 (en) * | 1997-05-22 | 2003-02-04 | G.D. Searle & Company | Substituted pyrazoles as p38 kinase inhibitors |
| GB9824310D0 (en) * | 1998-11-05 | 1998-12-30 | Univ London | Activators of soluble guanylate cyclase |
| AU2005276590B2 (en) * | 2004-08-27 | 2011-05-19 | Laboratorios Del Dr. Esteve, S.A. | Sigma receptor inhibitors |
| EP1634872A1 (en) * | 2004-08-27 | 2006-03-15 | Laboratorios Del Dr. Esteve, S.A. | Pyrazole derivatives as sigma receptor inhibitors |
-
2006
- 2006-03-02 EP EP06004288A patent/EP1829873A1/en not_active Withdrawn
-
2007
- 2007-03-02 JP JP2008556726A patent/JP2009528318A/ja active Pending
- 2007-03-02 WO PCT/EP2007/001827 patent/WO2007098964A2/en not_active Ceased
- 2007-03-02 ES ES07723022.5T patent/ES2572985T3/es active Active
- 2007-03-02 CA CA002640754A patent/CA2640754A1/en not_active Abandoned
- 2007-03-02 CN CN2007800071787A patent/CN101395152B/zh not_active Expired - Fee Related
- 2007-03-02 US US12/281,246 patent/US8138186B2/en not_active Expired - Fee Related
- 2007-03-02 MX MX2008011019A patent/MX2008011019A/es active IP Right Grant
- 2007-03-02 EP EP07723022.5A patent/EP1996580B1/en not_active Not-in-force
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