AU2003288159B2 - Asimadoline derivatives comprising covalently bonded acids - Google Patents

Asimadoline derivatives comprising covalently bonded acids Download PDF

Info

Publication number
AU2003288159B2
AU2003288159B2 AU2003288159A AU2003288159A AU2003288159B2 AU 2003288159 B2 AU2003288159 B2 AU 2003288159B2 AU 2003288159 A AU2003288159 A AU 2003288159A AU 2003288159 A AU2003288159 A AU 2003288159A AU 2003288159 B2 AU2003288159 B2 AU 2003288159B2
Authority
AU
Australia
Prior art keywords
acid
compound
salt
diseases
solvate
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.)
Ceased
Application number
AU2003288159A
Other languages
English (en)
Other versions
AU2003288159A1 (en
Inventor
Christoph Seyfried
Matthias Wiesner
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 AU2003288159A1 publication Critical patent/AU2003288159A1/en
Assigned to TIOGA PHARMACEUTICALS, INC. reassignment TIOGA PHARMACEUTICALS, INC. Request for Assignment Assignors: MERCK PATENT GMBH
Application granted granted Critical
Publication of AU2003288159B2 publication Critical patent/AU2003288159B2/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

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)
AU2003288159A 2002-12-17 2003-11-25 Asimadoline derivatives comprising covalently bonded acids Ceased AU2003288159B2 (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
AU2003288159A1 AU2003288159A1 (en) 2004-07-09
AU2003288159B2 true AU2003288159B2 (en) 2010-05-20

Family

ID=32403913

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2003288159A Ceased AU2003288159B2 (en) 2002-12-17 2003-11-25 Asimadoline derivatives comprising 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

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0569802A1 (de) * 1992-05-09 1993-11-18 MERCK PATENT GmbH Arylacetamide

Family Cites Families (22)

* 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
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

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0569802A1 (de) * 1992-05-09 1993-11-18 MERCK PATENT GmbH Arylacetamide

Also Published As

Publication number Publication date
CA2510167C (en) 2011-05-24
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
US7915228B2 (en) 2011-03-29
CA2510167A1 (en) 2004-07-01
DK1572640T3 (da) 2013-02-11

Similar Documents

Publication Publication Date Title
US7915228B2 (en) Derivatives of asimadoline with covalently bonded acids
JP5308056B2 (ja) 炎症性腹部疾患のためのカッパ−アヘン製剤作働薬
JP2023012547A (ja) Ｇｉｐ受容体活性化ペプチド
WO2011083304A1 (en) Prodrugs of opioids and uses thereof
KR20050072809A (ko) 아세트산 아닐리드 유도체를 유효성분으로 하는 과활동방광 치료제
EA017429B1 (ru) Циклические аминные соединения
JP2009046501A (ja) Ｎ−メチル−ｎ−［（１ｓ）−１−フェニル−２−｛（３ｓ）−３−ヒドロキシピロリジン−１−イル｝エチル］−２，２−ジフェニルアセトアミド
CN102159578A (zh) 四氢咪唑并[1,5-a]吡嗪衍生物的盐,其制备方法及其在医药上的应用
KR100358374B1 (ko) 5-ｈｔ3 및 5-ｈｔ4 매개된 질환에 유용한(+)-노르시사프라이드
WO2014142363A1 (en) Spiro azetidine isoxazole derivatives and their use as sstr5 antagonists
ZA200601228B (en) Kappa agonists, especially for the treatment and/or prophylaxis of irritable bowel syndrome
RU2349585C2 (ru) Стабильные модификации гидромалеата тегасерода
DE60001100T2 (de) Benzamid-derivate und sie enthaltende medikamente
TW202540152A (zh) 具有經修飾之離胺酸殘基之雜合肽化合物
WO2011147207A1 (zh) 六氢吡咯[3，4-b]吡咯衍生物、其制备方法及其用途
HK1080479B (en) Asimadoline derivatives comprising covalently bonded acids
DE69720518T2 (de) Neue derivate von n-substituierten pyrrolidin derivaten und deren herstellungsverfahren
CN108299397B (zh) 一种用于降血压的活性药物及其制备方法
CN116836216A (zh) 氟维司群衍生物及其制备方法和医药用途

Legal Events

Date Code Title Description
PC1 Assignment before grant (sect. 113)

Owner name: TIOGA PHARMACEUTICALS, INC.

Free format text: FORMER APPLICANT(S): MERCK PATENT GMBH

FGA Letters patent sealed or granted (standard patent)
MK14 Patent ceased section 143(a) (annual fees not paid) or expired