JP2011157375A5 - - Google Patents
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- Publication number
- JP2011157375A5 JP2011157375A5 JP2011079933A JP2011079933A JP2011157375A5 JP 2011157375 A5 JP2011157375 A5 JP 2011157375A5 JP 2011079933 A JP2011079933 A JP 2011079933A JP 2011079933 A JP2011079933 A JP 2011079933A JP 2011157375 A5 JP2011157375 A5 JP 2011157375A5
- Authority
- JP
- Japan
- Prior art keywords
- solvate
- salt
- derivative according
- appetite suppressant
- pain
- 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
- 150000003839 salts Chemical class 0.000 claims 14
- 239000012453 solvate Substances 0.000 claims 14
- 239000002830 appetite depressant Substances 0.000 claims 9
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 7
- 201000010099 disease Diseases 0.000 claims 6
- 238000004519 manufacturing process Methods 0.000 claims 5
- 208000002193 Pain Diseases 0.000 claims 4
- 239000003814 drug Substances 0.000 claims 4
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 claims 3
- 239000002253 acid Substances 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 230000002265 prevention Effects 0.000 claims 3
- KWGRBVOPPLSCSI-WPRPVWTQSA-N (-)-ephedrine Chemical compound CN[C@@H](C)[C@H](O)C1=CC=CC=C1 KWGRBVOPPLSCSI-WPRPVWTQSA-N 0.000 claims 2
- -1 (3S) -3- hydroxypyrrolidine-1-yl Chemical group 0.000 claims 2
- 208000008589 Obesity Diseases 0.000 claims 2
- QAOWNCQODCNURD-UHFFFAOYSA-N Sulfuric acid Chemical compound OS(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 claims 2
- 230000002378 acidificating effect Effects 0.000 claims 2
- 239000002671 adjuvant Substances 0.000 claims 2
- 208000022531 anorexia Diseases 0.000 claims 2
- DLNKOYKMWOXYQA-IONNQARKSA-N cathine Chemical compound C[C@H](N)[C@@H](O)C1=CC=CC=C1 DLNKOYKMWOXYQA-IONNQARKSA-N 0.000 claims 2
- 150000001875 compounds Chemical class 0.000 claims 2
- 206010061428 decreased appetite Diseases 0.000 claims 2
- 208000010643 digestive system disease Diseases 0.000 claims 2
- DLNKOYKMWOXYQA-UHFFFAOYSA-N dl-pseudophenylpropanolamine Natural products CC(N)C(O)C1=CC=CC=C1 DLNKOYKMWOXYQA-UHFFFAOYSA-N 0.000 claims 2
- 239000002552 dosage form Substances 0.000 claims 2
- 208000018685 gastrointestinal system disease Diseases 0.000 claims 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
- 208000027866 inflammatory disease Diseases 0.000 claims 2
- 230000002757 inflammatory effect Effects 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 235000020824 obesity Nutrition 0.000 claims 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims 2
- 239000000018 receptor agonist Substances 0.000 claims 2
- 229940044601 receptor agonist Drugs 0.000 claims 2
- 208000024891 symptom Diseases 0.000 claims 2
- WZLQYDXACAEGQZ-UHFFFAOYSA-N 6-[1-[2-[(2,2-diphenylacetyl)-methylamino]-2-phenylethyl]pyrrolidin-3-yl]oxy-3,4,5-trihydroxyoxane-2-carboxylic acid Chemical compound C=1C=CC=CC=1C(C=1C=CC=CC=1)C(=O)N(C)C(C=1C=CC=CC=1)CN(C1)CCC1OC1OC(C(O)=O)C(O)C(O)C1O WZLQYDXACAEGQZ-UHFFFAOYSA-N 0.000 claims 1
- 206010005052 Bladder irritation Diseases 0.000 claims 1
- 208000032841 Bulimia Diseases 0.000 claims 1
- 206010006550 Bulimia nervosa Diseases 0.000 claims 1
- 206010006895 Cachexia Diseases 0.000 claims 1
- 208000012661 Dyskinesia Diseases 0.000 claims 1
- 206010014020 Ear pain Diseases 0.000 claims 1
- 206010015958 Eye pain Diseases 0.000 claims 1
- IAJILQKETJEXLJ-UHFFFAOYSA-N Galacturonsaeure Natural products O=CC(O)C(O)C(O)C(O)C(O)=O IAJILQKETJEXLJ-UHFFFAOYSA-N 0.000 claims 1
- 206010018007 Gastrointestinal stenosis Diseases 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 102000003840 Opioid Receptors Human genes 0.000 claims 1
- 108090000137 Opioid Receptors Proteins 0.000 claims 1
- 208000007542 Paresis Diseases 0.000 claims 1
- NWAYMPWGUSKQRV-UHFFFAOYSA-N [1-[2-[(2-oxo-3,3-diphenylpropyl)amino]-2-phenylethyl]pyrrolidin-3-yl] hydrogen sulfate Chemical compound C1CN(CC1OS(=O)(=O)O)CC(C2=CC=CC=C2)NCC(=O)C(C3=CC=CC=C3)C4=CC=CC=C4 NWAYMPWGUSKQRV-UHFFFAOYSA-N 0.000 claims 1
- IAJILQKETJEXLJ-QTBDOELSSA-N aldehydo-D-glucuronic acid Chemical compound O=C[C@H](O)[C@@H](O)[C@H](O)[C@H](O)C(O)=O IAJILQKETJEXLJ-QTBDOELSSA-N 0.000 claims 1
- 125000005907 alkyl ester group Chemical class 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
- 229960003609 cathine Drugs 0.000 claims 1
- 230000001684 chronic effect Effects 0.000 claims 1
- KWGRBVOPPLSCSI-UHFFFAOYSA-N d-ephedrine Natural products CNC(C)C(O)C1=CC=CC=C1 KWGRBVOPPLSCSI-UHFFFAOYSA-N 0.000 claims 1
- 230000001079 digestive effect Effects 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 201000006549 dyspepsia Diseases 0.000 claims 1
- 229960002179 ephedrine Drugs 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 125000000524 functional group Chemical group 0.000 claims 1
- 210000001035 gastrointestinal tract Anatomy 0.000 claims 1
- 229940097043 glucuronic acid Drugs 0.000 claims 1
- 208000008384 ileus Diseases 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 210000000936 intestine Anatomy 0.000 claims 1
- 208000002551 irritable bowel syndrome Diseases 0.000 claims 1
- DKLYDESVXZKCFI-UHFFFAOYSA-N n,n-diphenylacetamide Chemical class C=1C=CC=CC=1N(C(=O)C)C1=CC=CC=C1 DKLYDESVXZKCFI-UHFFFAOYSA-N 0.000 claims 1
- DIZKGJLRHOCMTP-UHFFFAOYSA-N n-methyl-2,2-diphenylacetamide Chemical group C=1C=CC=CC=1C(C(=O)NC)C1=CC=CC=C1 DIZKGJLRHOCMTP-UHFFFAOYSA-N 0.000 claims 1
- 201000001119 neuropathy Diseases 0.000 claims 1
- 230000007823 neuropathy Effects 0.000 claims 1
- 229940127240 opiate Drugs 0.000 claims 1
- 208000033808 peripheral neuropathy Diseases 0.000 claims 1
- DLNKOYKMWOXYQA-APPZFPTMSA-N phenylpropanolamine Chemical group C[C@@H](N)[C@H](O)C1=CC=CC=C1 DLNKOYKMWOXYQA-APPZFPTMSA-N 0.000 claims 1
- 229960000395 phenylpropanolamine Drugs 0.000 claims 1
- JHHZLHWJQPUNKB-UHFFFAOYSA-N pyrrolidin-3-ol Chemical group OC1CCNC1 JHHZLHWJQPUNKB-UHFFFAOYSA-N 0.000 claims 1
- UNAANXDKBXWMLN-UHFFFAOYSA-N sibutramine Chemical compound C=1C=C(Cl)C=CC=1C1(C(N(C)C)CC(C)C)CCC1 UNAANXDKBXWMLN-UHFFFAOYSA-N 0.000 claims 1
- 229960004425 sibutramine Drugs 0.000 claims 1
- 210000002784 stomach Anatomy 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- 210000001635 urinary tract Anatomy 0.000 claims 1
Applications Claiming Priority (2)
| 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 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2004559717A Division 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 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2011157375A JP2011157375A (ja) | 2011-08-18 |
| JP2011157375A5 true JP2011157375A5 (enExample) | 2012-10-25 |
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 Before (1)
| 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 |
Country Status (14)
| Country | Link |
|---|---|
| US (3) | US7385065B2 (enExample) |
| EP (1) | EP1572640B1 (enExample) |
| JP (2) | JP5253709B2 (enExample) |
| AU (1) | AU2003288159B2 (enExample) |
| CA (1) | CA2510167C (enExample) |
| CY (1) | CY1113781T1 (enExample) |
| DE (1) | DE10259245A1 (enExample) |
| DK (1) | DK1572640T3 (enExample) |
| ES (1) | ES2401876T3 (enExample) |
| PE (1) | PE20040910A1 (enExample) |
| PT (1) | PT1572640E (enExample) |
| SI (1) | SI1572640T1 (enExample) |
| TW (1) | TWI335815B (enExample) |
| WO (1) | WO2004054970A1 (enExample) |
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 |
| US20080090859A1 (en) * | 2003-10-30 | 2008-04-17 | Tioga Pharmaceuticals, Inc. | Use of Selective Opiate Receptor Modulators In the Treatment Of Neuropathy |
| AU2008232954A1 (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 |
| EP3558300B1 (en) | 2016-12-21 | 2021-11-24 | Tioga Pharmaceuticals, Inc. | Solid pharmaceutical formulations of asimadoline |
| 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 |
| PT946157E (pt) * | 1996-12-16 | 2002-07-31 | Alcon Lab Inc | Utilizacao topica de agonistas kapa-opioides para o tratamento da dor ocular |
| AP2000001856A0 (en) * | 1997-12-24 | 2000-09-30 | Vertex Pharma | Prodrugs of aspartyl protease inhibitors. |
| 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 |
| JP4711600B2 (ja) * | 2001-01-26 | 2011-06-29 | シェーリング コーポレイション | シトステロール血症の処置のための置換アゼチジノン化合物の使用 |
| DE10116978A1 (de) * | 2001-04-05 | 2002-10-10 | Merck Patent Gmbh | Kappa-Opiatagonisten für die Behandlung von Erkrankungen der Blase |
| US6780891B2 (en) | 2001-11-30 | 2004-08-24 | Sepracor Inc. | Tramadol analogs and uses thereof |
| CN101310723A (zh) | 2002-05-17 | 2008-11-26 | 迪欧加药品公司 | 有效的选择性阿片受体调制剂化合物的用途 |
| 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 JP JP2004559717A patent/JP5253709B2/ja not_active Expired - Fee Related
- 2003-11-25 US US10/539,256 patent/US7385065B2/en not_active Expired - Fee Related
- 2003-11-25 WO PCT/EP2003/013206 patent/WO2004054970A1/de not_active Ceased
- 2003-11-25 DK DK03780043.0T patent/DK1572640T3/da active
- 2003-11-25 AU AU2003288159A patent/AU2003288159B2/en not_active Ceased
- 2003-11-25 EP EP03780043A patent/EP1572640B1/de not_active Expired - Lifetime
- 2003-11-25 CA CA2510167A patent/CA2510167C/en not_active Expired - Fee Related
- 2003-11-25 ES ES03780043T patent/ES2401876T3/es not_active Expired - Lifetime
- 2003-11-25 PT PT37800430T patent/PT1572640E/pt unknown
- 2003-11-25 SI SI200332242T patent/SI1572640T1/sl unknown
- 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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