JP2006511521A5 - - Google Patents
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- Publication number
- JP2006511521A5 JP2006511521A5 JP2004559717A JP2004559717A JP2006511521A5 JP 2006511521 A5 JP2006511521 A5 JP 2006511521A5 JP 2004559717 A JP2004559717 A JP 2004559717A JP 2004559717 A JP2004559717 A JP 2004559717A JP 2006511521 A5 JP2006511521 A5 JP 2006511521A5
- Authority
- JP
- Japan
- Prior art keywords
- group
- formula
- acid
- groups
- compound
- 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.)
- Granted
Links
- 150000001875 compounds Chemical class 0.000 claims description 12
- 150000003839 salts Chemical class 0.000 claims description 6
- 125000004432 carbon atom Chemical group C* 0.000 claims description 4
- 239000012453 solvate Substances 0.000 claims description 4
- 125000006239 protecting group Chemical group 0.000 claims description 3
- 125000000217 alkyl group Chemical group 0.000 claims description 2
- 238000004519 manufacturing process Methods 0.000 claims description 2
- 239000000651 prodrug Substances 0.000 claims description 2
- 229940002612 prodrug Drugs 0.000 claims description 2
- 239000002253 acid Substances 0.000 claims 3
- 238000000034 method Methods 0.000 claims 2
- ABLZXFCXXLZCGV-UHFFFAOYSA-N Phosphorous acid Chemical compound OP(O)=O ABLZXFCXXLZCGV-UHFFFAOYSA-N 0.000 claims 1
- 125000002252 acyl group Chemical group 0.000 claims 1
- JHLHNYVMZCADTC-LOSJGSFVSA-N asimadoline Chemical compound C([C@@H](N(C)C(=O)C(C=1C=CC=CC=1)C=1C=CC=CC=1)C=1C=CC=CC=1)N1CC[C@H](O)C1 JHLHNYVMZCADTC-LOSJGSFVSA-N 0.000 claims 1
- 125000000524 functional group Chemical group 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 229910021645 metal ion Inorganic materials 0.000 claims 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 1
- 125000000542 sulfonic acid group Chemical group 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 4
- 0 CN(C(C[C@](C1)O)*1CC1c2ccccc2)*1C(C(c1ccccc1)c1ccccc1)=O Chemical compound CN(C(C[C@](C1)O)*1CC1c2ccccc2)*1C(C(c1ccccc1)c1ccccc1)=O 0.000 description 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 description 2
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 2
- CGOWXHFQLCCWBS-RRPNLBNLSA-N [(3s)-1-[(2s)-2-[(2,2-diphenylacetyl)-methylamino]-2-phenylethyl]pyrrolidin-3-yl] acetate Chemical compound C([C@@H](N(C)C(=O)C(C=1C=CC=CC=1)C=1C=CC=CC=1)C=1C=CC=CC=1)N1CC[C@H](OC(C)=O)C1 CGOWXHFQLCCWBS-RRPNLBNLSA-N 0.000 description 1
- 239000004480 active ingredient Substances 0.000 description 1
- 125000003710 aryl alkyl group Chemical group 0.000 description 1
- 125000003118 aryl group Chemical group 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 230000010235 enterohepatic circulation Effects 0.000 description 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 1
- 230000003993 interaction Effects 0.000 description 1
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 description 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 1
- 125000004108 n-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 description 1
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 description 1
- 125000000636 p-nitrophenyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)[N+]([O-])=O 0.000 description 1
- 125000001037 p-tolyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)C([H])([H])[H] 0.000 description 1
- 239000000825 pharmaceutical preparation Substances 0.000 description 1
- 230000004962 physiological condition Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE10259245A DE10259245A1 (de) | 2002-12-17 | 2002-12-17 | Derivate des Asimadolins mit kovalent gebundenen Säuren |
| DE10259245.4 | 2002-12-17 | ||
| PCT/EP2003/013206 WO2004054970A1 (de) | 2002-12-17 | 2003-11-25 | Derivate des asimadolins mit kovalent gebundenen säuren |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011079933A Division JP2011157375A (ja) | 2002-12-17 | 2011-03-31 | 共有結合した酸を有するアシマドリンの誘導体 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2006511521A JP2006511521A (ja) | 2006-04-06 |
| JP2006511521A5 true JP2006511521A5 (https=) | 2007-01-18 |
| JP5253709B2 JP5253709B2 (ja) | 2013-07-31 |
Family
ID=32403913
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2004559717A Expired - Fee Related JP5253709B2 (ja) | 2002-12-17 | 2003-11-25 | 共有結合した酸を有するアシマドリンの誘導体 |
| JP2011079933A Pending JP2011157375A (ja) | 2002-12-17 | 2011-03-31 | 共有結合した酸を有するアシマドリンの誘導体 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011079933A Pending JP2011157375A (ja) | 2002-12-17 | 2011-03-31 | 共有結合した酸を有するアシマドリンの誘導体 |
Country Status (14)
| Country | Link |
|---|---|
| US (3) | US7385065B2 (https=) |
| EP (1) | EP1572640B1 (https=) |
| JP (2) | JP5253709B2 (https=) |
| AU (1) | AU2003288159B2 (https=) |
| CA (1) | CA2510167C (https=) |
| CY (1) | CY1113781T1 (https=) |
| DE (1) | DE10259245A1 (https=) |
| DK (1) | DK1572640T3 (https=) |
| ES (1) | ES2401876T3 (https=) |
| PE (1) | PE20040910A1 (https=) |
| PT (1) | PT1572640E (https=) |
| SI (1) | SI1572640T1 (https=) |
| TW (1) | TWI335815B (https=) |
| WO (1) | WO2004054970A1 (https=) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE10259245A1 (de) * | 2002-12-17 | 2004-07-01 | Merck Patent Gmbh | Derivate des Asimadolins mit kovalent gebundenen Säuren |
| EP1680115A1 (en) * | 2003-10-30 | 2006-07-19 | Tioga Pharmaceuticals, Inc. | Use of selective opiate receptor modulators in the treatment of neuropathy |
| CA2682608A1 (en) * | 2007-03-30 | 2008-10-09 | Tioga Pharmaceuticals, Inc. | Kappa-opiate agonists for the treatment of diarrhea-predominant and alternating irritable bowel syndrome |
| US9815824B2 (en) | 2013-06-28 | 2017-11-14 | Nektar Therapeutics | Kappa opioid agonists and uses thereof |
| ES2906979T3 (es) | 2016-12-21 | 2022-04-21 | Tioga Pharmaceuticals Inc | Formulaciones farmacéuticas sólidas de asimadolina |
| WO2019122361A1 (en) | 2017-12-22 | 2019-06-27 | Dr. August Wolff Gmbh & Co. Kg Arzneimittel | Asimadoline for use in treating pulmonary diseases, vascular diseases, and sepsis |
| EP3932390A1 (en) | 2020-07-02 | 2022-01-05 | Dr. August Wolff GmbH & Co. KG Arzneimittel | Topical gel formulation containing asimadoline |
Family Cites Families (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4760069A (en) | 1985-09-23 | 1988-07-26 | Nova Pharmaceutical Corporation | Oximes of oxymorphone, naltrexone and naloxone as potent, selective opioid receptor agonists and antagonists |
| US4889860A (en) | 1985-09-23 | 1989-12-26 | Nova Pharmaceutical Corporation | Oximes of oxymorphone, naltrexone and naloxone as potent, selective opioid receptor agonists and antagonists |
| US5300687A (en) | 1991-07-18 | 1994-04-05 | Ortho Pharmaceutical Corporation | Trifluoromethylbenzylphosphonates useful in treating osteoporosis |
| DE4215213A1 (de) | 1992-05-09 | 1993-11-11 | Merck Patent Gmbh | Arylacetamide |
| DE4425071C2 (de) | 1994-07-15 | 1996-08-29 | Degussa | Verfahren zur Herstellung optisch aktiver Pyrrolidine mit hoher Enantiomerenreinheit |
| DE19523502A1 (de) | 1995-06-28 | 1997-01-02 | Merck Patent Gmbh | Kappa-Opiatagonisten für entzündliche Darmerkrankungen |
| DE19531464A1 (de) | 1995-08-26 | 1997-02-27 | Merck Patent Gmbh | N-Methyl-N-[(1S-)-1-phenyl-2-((3S)-3-hydroxypyrrolidin 1-yl-)-ethyl]-2,2-diphenyl-acetamid |
| US6303611B1 (en) * | 1996-03-08 | 2001-10-16 | Adolor Corporation | Kappa agonist compounds and pharmaceutical formulations thereof |
| DE19647538A1 (de) | 1996-11-16 | 1998-05-20 | Merck Patent Gmbh | Verfahren zur Herstellung von enantiomerenreinem N-Methyl-N-[1-phenyl-2-(-3-hydroxypyrrolidin-1-yl)ethyl]-2,2-diphenylacetamid |
| ES2174337T3 (es) * | 1996-12-16 | 2002-11-01 | Alcon Lab Inc | Uso topico de los agonistas opioides kappa para el tratamiento del dolor ocular. |
| EA200000702A1 (ru) * | 1997-12-24 | 2000-12-25 | Вертекс Фармасьютикалз Инкорпорейтед | Пролекарства ингибиторов аспартилпротеаз |
| DE19827633A1 (de) | 1998-04-20 | 1999-10-21 | Merck Patent Gmbh | Verfahren zur Herstellung von enantiomerenreinem N-Methyl-N-[(1S)-1-phenyl-2-((3S)-3-hydroxypyrrolidin-1-yl)ethyl]-2,2-diphenylacetamid |
| DE19849650A1 (de) | 1998-10-29 | 2000-05-04 | Merck Patent Gmbh | Kappa-Opiatagonisten für die Behandlung des Irritable Bowel Syndroms (IBS) |
| US20020025948A1 (en) | 2000-06-23 | 2002-02-28 | Banks Bernard Joseph | 3-azabicyclo[3.1.0]hexane derivatives useful in therapy |
| GB0015562D0 (en) | 2000-06-23 | 2000-08-16 | Pfizer Ltd | Heterocycles |
| US6846831B2 (en) | 2000-08-15 | 2005-01-25 | Cpd, Llc | Method of treating the syndrome of lipodystrophy |
| US6262062B1 (en) | 2000-08-15 | 2001-07-17 | Cpd, Llc | Method of treating the syndrome of coronary heart disease risk factors in humans |
| US6569449B1 (en) | 2000-11-13 | 2003-05-27 | University Of Kentucky Research Foundation | Transdermal delivery of opioid antagonist prodrugs |
| DK1355644T3 (da) * | 2001-01-26 | 2006-10-23 | Schering Corp | Anvendelse af substituerede azetidinonforbindelser til behandling af sitosterolæmi |
| DE10116978A1 (de) * | 2001-04-05 | 2002-10-10 | Merck Patent Gmbh | Kappa-Opiatagonisten für die Behandlung von Erkrankungen der Blase |
| WO2003048113A1 (en) | 2001-11-30 | 2003-06-12 | Sepracor Inc. | Tramadol analogs and uses thereof |
| WO2003097051A2 (en) * | 2002-05-17 | 2003-11-27 | Merck Patent Gmbh | Use of compounds that are effective as selective opiate receptor modulators |
| DE10259245A1 (de) * | 2002-12-17 | 2004-07-01 | Merck Patent Gmbh | Derivate des Asimadolins mit kovalent gebundenen Säuren |
-
2002
- 2002-12-17 DE DE10259245A patent/DE10259245A1/de not_active Withdrawn
-
2003
- 2003-11-25 SI SI200332242T patent/SI1572640T1/sl unknown
- 2003-11-25 JP JP2004559717A patent/JP5253709B2/ja not_active Expired - Fee Related
- 2003-11-25 DK DK03780043.0T patent/DK1572640T3/da active
- 2003-11-25 PT PT37800430T patent/PT1572640E/pt unknown
- 2003-11-25 WO PCT/EP2003/013206 patent/WO2004054970A1/de not_active Ceased
- 2003-11-25 EP EP03780043A patent/EP1572640B1/de not_active Expired - Lifetime
- 2003-11-25 ES ES03780043T patent/ES2401876T3/es not_active Expired - Lifetime
- 2003-11-25 AU AU2003288159A patent/AU2003288159B2/en not_active Ceased
- 2003-11-25 CA CA2510167A patent/CA2510167C/en not_active Expired - Fee Related
- 2003-11-25 US US10/539,256 patent/US7385065B2/en not_active Expired - Fee Related
- 2003-12-10 PE PE2003001254A patent/PE20040910A1/es not_active Application Discontinuation
- 2003-12-11 TW TW092135046A patent/TWI335815B/zh not_active IP Right Cessation
-
2007
- 2007-04-02 US US11/732,309 patent/US20070179098A1/en not_active Abandoned
-
2008
- 2008-06-02 US US12/131,836 patent/US7915228B2/en not_active Expired - Fee Related
-
2011
- 2011-03-31 JP JP2011079933A patent/JP2011157375A/ja active Pending
-
2013
- 2013-02-04 CY CY20131100097T patent/CY1113781T1/el unknown
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