DE10259245A1 - Derivate des Asimadolins mit kovalent gebundenen Säuren - Google Patents
Derivate des Asimadolins mit kovalent gebundenen Säuren Download PDFInfo
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- DE10259245A1 DE10259245A1 DE10259245A DE10259245A DE10259245A1 DE 10259245 A1 DE10259245 A1 DE 10259245A1 DE 10259245 A DE10259245 A DE 10259245A DE 10259245 A DE10259245 A DE 10259245A DE 10259245 A1 DE10259245 A1 DE 10259245A1
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- Prior art keywords
- acid
- derivatives
- derivative according
- acids
- salt
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- 239000002253 acid Substances 0.000 title claims abstract description 107
- 150000007513 acids Chemical class 0.000 title claims abstract description 30
- 150000003839 salts Chemical class 0.000 claims abstract description 58
- 238000000034 method Methods 0.000 claims abstract description 40
- -1 (3S) -3-hydroxypyrrolidin-1-yl Chemical group 0.000 claims abstract description 39
- 238000011282 treatment Methods 0.000 claims abstract description 37
- 239000012453 solvate Substances 0.000 claims abstract description 28
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract description 27
- 238000002360 preparation method Methods 0.000 claims abstract description 26
- 239000003814 drug Substances 0.000 claims abstract description 23
- 201000010099 disease Diseases 0.000 claims abstract description 21
- 230000008569 process Effects 0.000 claims abstract description 19
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 15
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- 239000000651 prodrug Substances 0.000 claims abstract description 11
- 229940002612 prodrug Drugs 0.000 claims abstract description 11
- 150000001875 compounds Chemical class 0.000 claims description 79
- JHLHNYVMZCADTC-LOSJGSFVSA-N asimadoline Chemical class 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 description 29
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 29
- QAOWNCQODCNURD-UHFFFAOYSA-N Sulfuric acid Chemical compound OS(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 claims description 24
- 125000006239 protecting group Chemical group 0.000 claims description 23
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- DLNKOYKMWOXYQA-UHFFFAOYSA-N dl-pseudophenylpropanolamine Natural products CC(N)C(O)C1=CC=CC=C1 DLNKOYKMWOXYQA-UHFFFAOYSA-N 0.000 claims description 6
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- 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 claims description 5
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- DLNKOYKMWOXYQA-IONNQARKSA-N cathine Chemical compound C[C@H](N)[C@@H](O)C1=CC=CC=C1 DLNKOYKMWOXYQA-IONNQARKSA-N 0.000 claims description 4
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- JHHZLHWJQPUNKB-UHFFFAOYSA-N pyrrolidin-3-ol Chemical group OC1CCNC1 JHHZLHWJQPUNKB-UHFFFAOYSA-N 0.000 claims description 3
- 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 description 2
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- 150000008043 acidic salts Chemical group 0.000 claims description 2
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- 239000000969 carrier Substances 0.000 claims description 2
- KWGRBVOPPLSCSI-UHFFFAOYSA-N d-ephedrine Natural products CNC(C)C(O)C1=CC=CC=C1 KWGRBVOPPLSCSI-UHFFFAOYSA-N 0.000 claims description 2
- XXEPPPIWZFICOJ-UHFFFAOYSA-N diethylpropion Chemical compound CCN(CC)C(C)C(=O)C1=CC=CC=C1 XXEPPPIWZFICOJ-UHFFFAOYSA-N 0.000 claims description 2
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- 239000008177 pharmaceutical agent Substances 0.000 claims description 2
- DLNKOYKMWOXYQA-APPZFPTMSA-N phenylpropanolamine Chemical compound C[C@@H](N)[C@H](O)C1=CC=CC=C1 DLNKOYKMWOXYQA-APPZFPTMSA-N 0.000 claims description 2
- 229960000395 phenylpropanolamine Drugs 0.000 claims description 2
- ABLZXFCXXLZCGV-UHFFFAOYSA-N phosphonic acid group Chemical group P(O)(O)=O ABLZXFCXXLZCGV-UHFFFAOYSA-N 0.000 claims description 2
- 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 description 2
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- 230000036262 stenosis Effects 0.000 claims 1
- 208000037804 stenosis Diseases 0.000 claims 1
- 210000001635 urinary tract Anatomy 0.000 claims 1
- DKLYDESVXZKCFI-UHFFFAOYSA-N n,n-diphenylacetamide Chemical compound C=1C=CC=CC=1N(C(=O)C)C1=CC=CC=C1 DKLYDESVXZKCFI-UHFFFAOYSA-N 0.000 abstract 1
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 24
- HEMHJVSKTPXQMS-UHFFFAOYSA-M sodium hydroxide Inorganic materials [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 22
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 18
- 238000006243 chemical reaction Methods 0.000 description 18
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- 230000000694 effects Effects 0.000 description 16
- RTZKZFJDLAIYFH-UHFFFAOYSA-N ether Substances CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 16
- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 description 15
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- 150000002148 esters Chemical class 0.000 description 11
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 description 10
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- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 description 9
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 9
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 9
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- IAJILQKETJEXLJ-UHFFFAOYSA-N Galacturonsaeure Natural products O=CC(O)C(O)C(O)C(O)C(O)=O IAJILQKETJEXLJ-UHFFFAOYSA-N 0.000 description 8
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- 208000003251 Pruritus Diseases 0.000 description 8
- DTQVDTLACAAQTR-UHFFFAOYSA-N Trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F DTQVDTLACAAQTR-UHFFFAOYSA-N 0.000 description 8
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- 239000000243 solution Substances 0.000 description 7
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- 125000003118 aryl group Chemical group 0.000 description 6
- XBDQKXXYIPTUBI-UHFFFAOYSA-N dimethylselenoniopropionate Natural products CCC(O)=O XBDQKXXYIPTUBI-UHFFFAOYSA-N 0.000 description 6
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- TWBYWOBDOCUKOW-UHFFFAOYSA-N isonicotinic acid Chemical compound OC(=O)C1=CC=NC=C1 TWBYWOBDOCUKOW-UHFFFAOYSA-N 0.000 description 6
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- 230000008733 trauma Effects 0.000 description 1
- 229960002622 triacetin Drugs 0.000 description 1
- YNJBWRMUSHSURL-UHFFFAOYSA-N trichloroacetic acid Chemical compound OC(=O)C(Cl)(Cl)Cl YNJBWRMUSHSURL-UHFFFAOYSA-N 0.000 description 1
- 235000015112 vegetable and seed oil Nutrition 0.000 description 1
- 239000008158 vegetable oil Substances 0.000 description 1
- 239000011782 vitamin Substances 0.000 description 1
- 229940088594 vitamin Drugs 0.000 description 1
- 235000013343 vitamin Nutrition 0.000 description 1
- 229930003231 vitamin Natural products 0.000 description 1
- 230000008673 vomiting Effects 0.000 description 1
- 238000005406 washing Methods 0.000 description 1
- 239000000080 wetting agent Substances 0.000 description 1
- 238000010626 work up procedure Methods 0.000 description 1
- 108020001588 κ-opioid receptors Proteins 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no 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
- C07D207/12—Oxygen or sulfur atoms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/12—Antidiarrhoeals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/10—Drugs for disorders of the urinary system of the bladder
-
- 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
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
-
- 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
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/16—Otologicals
-
- 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
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Urology & Nephrology (AREA)
- Pain & Pain Management (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Rheumatology (AREA)
- Obesity (AREA)
- Psychology (AREA)
- Addiction (AREA)
- Psychiatry (AREA)
- Ophthalmology & Optometry (AREA)
- Nutrition Science (AREA)
- Child & Adolescent Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Pyrrole Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Saccharide Compounds (AREA)
Priority Applications (18)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE10259245A DE10259245A1 (de) | 2002-12-17 | 2002-12-17 | Derivate des Asimadolins mit kovalent gebundenen Säuren |
| AU2003288159A AU2003288159B2 (en) | 2002-12-17 | 2003-11-25 | Asimadoline derivatives comprising covalently bonded acids |
| HK06103233.5A HK1080479B (en) | 2002-12-17 | 2003-11-25 | Asimadoline derivatives comprising covalently bonded acids |
| PCT/EP2003/013206 WO2004054970A1 (de) | 2002-12-17 | 2003-11-25 | Derivate des asimadolins mit kovalent gebundenen säuren |
| PT37800430T PT1572640E (pt) | 2002-12-17 | 2003-11-25 | Derivados da asimadolina que compreendem ácidos ligados covalentemente |
| ES03780043T ES2401876T3 (es) | 2002-12-17 | 2003-11-25 | Derivados de asimadolina con ácidos unidos covalentemente |
| JP2004559717A 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 |
| DK03780043.0T DK1572640T3 (da) | 2002-12-17 | 2003-11-25 | Asimadolinderivater omfattende kovalent bundne syrer |
| EP03780043A EP1572640B1 (de) | 2002-12-17 | 2003-11-25 | Derivate des asimadolins mit kovalent gebundenen saeuren |
| SI200332242T SI1572640T1 (sl) | 2002-12-17 | 2003-11-25 | Asimadolinski derivati, ki vsebujejo kovalentno vezane kisline |
| US10/539,256 US7385065B2 (en) | 2002-12-17 | 2003-11-25 | Derivatives of asimadoline with covalently bonded acids |
| CA2510167A CA2510167C (en) | 2002-12-17 | 2003-11-25 | Derivatives of asimadoline with covalently bonded acids |
| PE2003001254A PE20040910A1 (es) | 2002-12-17 | 2003-12-10 | Derivados de asimadolina con acidos unidos covalentemente |
| TW092135046A TWI335815B (en) | 2002-12-17 | 2003-12-11 | Derivatives of asimadoline with covalently bonded acids |
| US11/732,309 US20070179098A1 (en) | 2002-12-17 | 2007-04-02 | Treatment of functional dyspepsia using asimadoline |
| US12/131,836 US7915228B2 (en) | 2002-12-17 | 2008-06-02 | Derivatives of asimadoline with covalently bonded acids |
| JP2011079933A 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 |
| CY20131100097T CY1113781T1 (el) | 2002-12-17 | 2013-02-04 | Παραγωγα της ασιμαδολινης με ομοιοπολικα συνδεδεμενα οξεα |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE10259245A DE10259245A1 (de) | 2002-12-17 | 2002-12-17 | Derivate des Asimadolins mit kovalent gebundenen Säuren |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| DE10259245A1 true DE10259245A1 (de) | 2004-07-01 |
Family
ID=32403913
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DE10259245A Withdrawn DE10259245A1 (de) | 2002-12-17 | 2002-12-17 | Derivate des Asimadolins mit kovalent gebundenen Säuren |
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 |
| US20080090859A1 (en) * | 2003-10-30 | 2008-04-17 | Tioga Pharmaceuticals, Inc. | Use of Selective Opiate Receptor Modulators In the Treatment Of Neuropathy |
| CN101677997B (zh) * | 2007-03-30 | 2012-05-09 | 泰奥加制药公司 | 用于治疗腹泻型和交替型肠易激综合征的κ-阿片剂激动剂 |
| JP6577943B2 (ja) * | 2013-06-28 | 2019-09-18 | ネクター セラピューティクス | κオピオイド作動薬及びその使用 |
| 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 |
| ES2174337T3 (es) * | 1996-12-16 | 2002-11-01 | Alcon Lab Inc | Uso topico de los agonistas opioides kappa para el tratamiento del dolor ocular. |
| EE200000386A (et) | 1997-12-24 | 2001-12-17 | Vertex Pharmaceuticals Incorporated | Aspartüülproteaasi inhibiitorite eelravimid |
| 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) |
| GB0015562D0 (en) | 2000-06-23 | 2000-08-16 | Pfizer Ltd | Heterocycles |
| US20020025948A1 (en) | 2000-06-23 | 2002-02-28 | Banks Bernard Joseph | 3-azabicyclo[3.1.0]hexane derivatives useful in therapy |
| US6262062B1 (en) | 2000-08-15 | 2001-07-17 | Cpd, Llc | Method of treating the syndrome of coronary heart disease risk factors in humans |
| US6846831B2 (en) | 2000-08-15 | 2005-01-25 | Cpd, Llc | Method of treating the syndrome of lipodystrophy |
| US6569449B1 (en) | 2000-11-13 | 2003-05-27 | University Of Kentucky Research Foundation | Transdermal delivery of opioid antagonist prodrugs |
| AR035533A1 (es) * | 2001-01-26 | 2004-06-02 | Schering Corp | Uso de por lo menos un inhibidor de la absorcion de los esteroles o sus sales, solvatos, prodrogas farmaceuticamente aceptables o mezclas de los mismos para la preparacion de un medicamento para el tratamiento de la sitosterolemia, composiciones farmaceuticas, el uso de dichas composiciones para la |
| 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 |
| US20050176746A1 (en) | 2002-05-17 | 2005-08-11 | Frank Weber | 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 PT PT37800430T patent/PT1572640E/pt unknown
- 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 JP JP2004559717A patent/JP5253709B2/ja not_active Expired - Fee Related
- 2003-11-25 SI SI200332242T patent/SI1572640T1/sl unknown
- 2003-11-25 US US10/539,256 patent/US7385065B2/en not_active Expired - Fee Related
- 2003-11-25 ES ES03780043T patent/ES2401876T3/es not_active Expired - Lifetime
- 2003-11-25 WO PCT/EP2003/013206 patent/WO2004054970A1/de not_active Ceased
- 2003-11-25 AU AU2003288159A patent/AU2003288159B2/en not_active Ceased
- 2003-11-25 DK DK03780043.0T patent/DK1572640T3/da active
- 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
Also Published As
| Publication number | Publication date |
|---|---|
| JP5253709B2 (ja) | 2013-07-31 |
| US7385065B2 (en) | 2008-06-10 |
| EP1572640B1 (de) | 2012-11-07 |
| ES2401876T3 (es) | 2013-04-25 |
| JP2006511521A (ja) | 2006-04-06 |
| SI1572640T1 (sl) | 2013-03-29 |
| TWI335815B (en) | 2011-01-11 |
| HK1080479A1 (en) | 2006-04-28 |
| US20080234209A1 (en) | 2008-09-25 |
| PT1572640E (pt) | 2013-02-15 |
| CA2510167C (en) | 2011-05-24 |
| CA2510167A1 (en) | 2004-07-01 |
| US20070179098A1 (en) | 2007-08-02 |
| EP1572640A1 (de) | 2005-09-14 |
| CY1113781T1 (el) | 2016-07-27 |
| AU2003288159A1 (en) | 2004-07-09 |
| US7915228B2 (en) | 2011-03-29 |
| JP2011157375A (ja) | 2011-08-18 |
| DK1572640T3 (da) | 2013-02-11 |
| TW200418459A (en) | 2004-10-01 |
| WO2004054970A1 (de) | 2004-07-01 |
| AU2003288159B2 (en) | 2010-05-20 |
| US20060122255A1 (en) | 2006-06-08 |
| PE20040910A1 (es) | 2004-12-02 |
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