CA2510167C - Derivatives of asimadoline with covalently bonded acids - Google Patents

Derivatives of asimadoline with covalently bonded acids Download PDF

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Publication number
CA2510167C
CA2510167C CA2510167A CA2510167A CA2510167C CA 2510167 C CA2510167 C CA 2510167C CA 2510167 A CA2510167 A CA 2510167A CA 2510167 A CA2510167 A CA 2510167A CA 2510167 C CA2510167 C CA 2510167C
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CA
Canada
Prior art keywords
acid
compound
salt
pain
group
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.)
Expired - Fee Related
Application number
CA2510167A
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English (en)
French (fr)
Other versions
CA2510167A1 (en
Inventor
Matthias Wiesner
Christoph Seyfried
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Tioga Pharmaceuticals Inc
Original Assignee
Tioga Pharmaceuticals Inc
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Tioga Pharmaceuticals Inc filed Critical Tioga Pharmaceuticals Inc
Publication of CA2510167A1 publication Critical patent/CA2510167A1/en
Application granted granted Critical
Publication of CA2510167C publication Critical patent/CA2510167C/en
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

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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)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Diabetes (AREA)
  • Addiction (AREA)
  • Psychiatry (AREA)
  • Ophthalmology & Optometry (AREA)
  • Child & Adolescent Psychology (AREA)
  • Rheumatology (AREA)
  • Psychology (AREA)
  • Obesity (AREA)
  • Nutrition Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
CA2510167A 2002-12-17 2003-11-25 Derivatives of asimadoline with covalently bonded acids Expired - Fee Related CA2510167C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
DE10259245.4 2002-12-17
DE10259245A DE10259245A1 (de) 2002-12-17 2002-12-17 Derivate des Asimadolins mit kovalent gebundenen Säuren
PCT/EP2003/013206 WO2004054970A1 (de) 2002-12-17 2003-11-25 Derivate des asimadolins mit kovalent gebundenen säuren

Publications (2)

Publication Number Publication Date
CA2510167A1 CA2510167A1 (en) 2004-07-01
CA2510167C true CA2510167C (en) 2011-05-24

Family

ID=32403913

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2510167A Expired - Fee Related CA2510167C (en) 2002-12-17 2003-11-25 Derivatives of asimadoline with covalently bonded acids

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)

* Cited by examiner, † Cited by third party
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
JP2007509865A (ja) * 2003-10-30 2007-04-19 ティオガ ファーマシュウティカルズ，インコーポレイテッド 神経障害の治療における選択的オピエート受容体調節物質の使用
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
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)

* Cited by examiner, † Cited by third party
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
CA2275167C (en) * 1996-12-16 2008-10-28 Alcon Laboratories, Inc. The topical use of kappa opioid agonists to treat ocular pain
EP1042280A2 (en) * 1997-12-24 2000-10-11 Vertex Pharmaceuticals Incorporated 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
KR20070120617A (ko) * 2001-01-26 2007-12-24 쉐링 코포레이션 치환된 아제티딘온 화합물을 포함하는 약제학적 조성물
DE10116978A1 (de) * 2001-04-05 2002-10-10 Merck Patent Gmbh Kappa-Opiatagonisten für die Behandlung von Erkrankungen der Blase
AU2002364517A1 (en) 2001-11-30 2003-06-17 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

Also Published As

Publication number Publication date
JP2011157375A (ja) 2011-08-18
CY1113781T1 (el) 2016-07-27
HK1080479A1 (en) 2006-04-28
EP1572640A1 (de) 2005-09-14
US20080234209A1 (en) 2008-09-25
EP1572640B1 (de) 2012-11-07
WO2004054970A1 (de) 2004-07-01
US20070179098A1 (en) 2007-08-02
JP5253709B2 (ja) 2013-07-31
US20060122255A1 (en) 2006-06-08
ES2401876T3 (es) 2013-04-25
PT1572640E (pt) 2013-02-15
DE10259245A1 (de) 2004-07-01
JP2006511521A (ja) 2006-04-06
AU2003288159A1 (en) 2004-07-09
SI1572640T1 (sl) 2013-03-29
TWI335815B (en) 2011-01-11
US7385065B2 (en) 2008-06-10
TW200418459A (en) 2004-10-01
PE20040910A1 (es) 2004-12-02
AU2003288159B2 (en) 2010-05-20
US7915228B2 (en) 2011-03-29
CA2510167A1 (en) 2004-07-01
DK1572640T3 (da) 2013-02-11

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MKLA Lapsed

Effective date: 20151125