CA2528323C - 2-hydroxymethyl-3,4,5-trihydroxy-1-benzilpiperidine derivatives as inhibitors of glucosylceramide - Google Patents

2-hydroxymethyl-3,4,5-trihydroxy-1-benzilpiperidine derivatives as inhibitors of glucosylceramide Download PDF

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Publication number
CA2528323C
CA2528323C CA2528323A CA2528323A CA2528323C CA 2528323 C CA2528323 C CA 2528323C CA 2528323 A CA2528323 A CA 2528323A CA 2528323 A CA2528323 A CA 2528323A CA 2528323 C CA2528323 C CA 2528323C
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Prior art keywords
disease
treatment
compound
compound defined
manufacture
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Expired - Fee Related
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CA2528323A
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English (en)
French (fr)
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CA2528323A1 (en
Inventor
Michael Glen Orchard
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Idorsia Pharmaceuticals Ltd
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Actelion Pharmaceuticals Ltd
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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
    • C07D211/40—Oxygen atoms
    • C07D211/44—Oxygen atoms attached in position 4
    • C07D211/46—Oxygen atoms attached in position 4 having a hydrogen atom as the second substituent in position 4
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • 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
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/16—Masculine contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P25/08—Antiepileptics; Anticonvulsants
    • 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
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Immunology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Cardiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Emergency Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Vascular Medicine (AREA)
  • Reproductive Health (AREA)
CA2528323A 2003-06-13 2004-06-09 2-hydroxymethyl-3,4,5-trihydroxy-1-benzilpiperidine derivatives as inhibitors of glucosylceramide Expired - Fee Related CA2528323C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GBGB0313678.5A GB0313678D0 (en) 2003-06-13 2003-06-13 Novel compounds
GB0313678.5 2003-06-13
PCT/GB2004/002451 WO2004111002A1 (en) 2003-06-13 2004-06-09 2-hydroxymethyl-3,4,5-trihydroxy-1-benzilpiperidine derivatives as inhibitors of glucosylceramide

Publications (2)

Publication Number Publication Date
CA2528323A1 CA2528323A1 (en) 2004-12-23
CA2528323C true CA2528323C (en) 2012-07-31

Family

ID=27590019

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2528323A Expired - Fee Related CA2528323C (en) 2003-06-13 2004-06-09 2-hydroxymethyl-3,4,5-trihydroxy-1-benzilpiperidine derivatives as inhibitors of glucosylceramide

Country Status (10)

Country Link
US (1) US8071780B2 (enExample)
EP (1) EP1636186A1 (enExample)
JP (1) JP4780785B2 (enExample)
CN (1) CN100422149C (enExample)
AU (1) AU2004247469B2 (enExample)
BR (1) BRPI0411308A8 (enExample)
CA (1) CA2528323C (enExample)
GB (1) GB0313678D0 (enExample)
IL (1) IL172542A (enExample)
WO (1) WO2004111002A1 (enExample)

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GB0100889D0 (en) 2001-01-12 2001-02-21 Oxford Glycosciences Uk Ltd Compounds
ES2393331T3 (es) * 2002-07-17 2012-12-20 Actelion Pharmaceuticals Ltd. Derivados de piperidintriol como inhibidores de la glucosiliceramida sintasa
AU2003248960B2 (en) * 2002-07-17 2009-06-25 Idorsia Pharmaceuticals Ltd Piperidinetriol derivatives as inhibitors of glycosylceramidsynthase
GB0313678D0 (en) 2003-06-13 2003-07-16 Oxford Glycosciences Uk Ltd Novel compounds
GB0313677D0 (en) * 2003-06-13 2003-07-16 Oxford Glycosciences Uk Ltd Novel compound
BRPI0517701A8 (pt) * 2004-11-10 2018-01-23 Genzyme Corp métodos de tratamento de diabetes mellitus
ES2546181T3 (es) * 2006-05-09 2015-09-21 Genzyme Corporation Métodos de tratar la enfermedad del hígado graso mediante inhibición de la síntesis de glucoesfingolípidos
GB0614947D0 (en) * 2006-07-27 2006-09-06 Isis Innovation Epitope reduction therapy
EP2594565B1 (en) * 2007-05-31 2018-10-24 Genzyme Corporation 2-acylaminopropanol-type glucosylceramide synthase inhibitors
GB0712494D0 (en) * 2007-06-27 2007-08-08 Isis Innovation Substrate reduction therapy
KR101640263B1 (ko) 2007-10-05 2016-07-15 젠자임 코포레이션 세라마이드 유도체로 다낭성 신장질환을 치료하는 방법
JP2011529500A (ja) * 2008-07-28 2011-12-08 ジェンザイム コーポレーション 虚脱性糸球体症および他の糸球体疾患の処置のためのグルコシルセラミドシンターゼ阻害
CN102271678B (zh) * 2008-10-03 2017-06-30 简詹姆公司 2‑酰胺基丙醇型葡糖神经酰胺合成酶抑制剂
US12612380B2 (en) 2019-05-10 2026-04-28 Alectos Therapeutics 1Nc Non-lysosomal glucosylceramidase inhibitors and uses thereof
PE20231423A1 (es) 2020-05-07 2023-09-13 Alectos Therapeutics Inc Inhibidores de glucosilceramidasa no lisosomal y los usos de los mismos

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NO154918C (no) * 1977-08-27 1987-01-14 Bayer Ag Analogifremgangsmaate til fremstilling av terapeutisk aktive derivater av 3,4,5-trihydroksypiperidin.
DE3007078A1 (de) * 1980-02-26 1981-09-10 Bayer Ag, 5090 Leverkusen Neue derivate von 3,4,5-trihydroxypiperidin, verfahren zu ihrer herstellung und ihre verwendung als arzneimittel sowie in der tierernaehrung
DE3024901A1 (de) 1980-07-01 1982-01-28 Bayer Ag, 5090 Leverkusen Herbizide mittel auf basis von piperidin-derivaten
DE3247615A1 (de) * 1982-12-23 1984-07-05 Hoechst Ag, 6230 Frankfurt Substituierte phenylsulfonyloxybenzimidazolcarbaminate, verfahren zu ihrer herstellung und ihre verwendung als arzneimittel
DE3737523A1 (de) * 1987-11-05 1989-05-18 Bayer Ag Verwendung von substituierten hydroxypiperidinen als antivirale mittel
US5003072A (en) * 1988-11-03 1991-03-26 G. D. Searle & Co. 1,5-dideoxy-1,5-imino-D-glucitol derivatives
JPH02306962A (ja) 1989-05-19 1990-12-20 Meiji Seika Kaisha Ltd 新規n―置換―1―デオキシノジリマイシン誘導体及びそれを含有する癌細胞転移抑制剤
JPH0324057A (ja) 1989-06-22 1991-02-01 Tosoh Corp ポリヒドロキシピペリジン類及びその製造法
WO1991003242A1 (en) 1989-09-07 1991-03-21 Nippon Shinyaku Co., Ltd. Antiviral drug
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US5276120A (en) * 1991-05-30 1994-01-04 The Scripps Research Institute Process for forming omega-deuxy-azasugars
JP3506434B2 (ja) 1993-05-05 2004-03-15 ロシュ ダイアグノスティックス ゲーエムベーハー ブレビバクテリウム・ステロリカム由来のコレステロールオキシダーゼ
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GB0100889D0 (en) * 2001-01-12 2001-02-21 Oxford Glycosciences Uk Ltd Compounds
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DE60037664T2 (de) 1999-08-10 2008-12-24 The Chancellor, Masters And Scholars Of The University Of Oxford Langkettige n-alkyl verbindungen und deren oxa-derivate zur verwendung als anitvirale mittel
US7256005B2 (en) * 1999-08-10 2007-08-14 The Chancellor, Masters And Scholars Of The University Of Oxford Methods for identifying iminosugar derivatives that inhibit HCV p7 ion channel activity
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AU2003248960B2 (en) * 2002-07-17 2009-06-25 Idorsia Pharmaceuticals Ltd Piperidinetriol derivatives as inhibitors of glycosylceramidsynthase
ES2393331T3 (es) 2002-07-17 2012-12-20 Actelion Pharmaceuticals Ltd. Derivados de piperidintriol como inhibidores de la glucosiliceramida sintasa
GB0313678D0 (en) 2003-06-13 2003-07-16 Oxford Glycosciences Uk Ltd Novel compounds
GB0313677D0 (en) * 2003-06-13 2003-07-16 Oxford Glycosciences Uk Ltd Novel compound
GB0400812D0 (en) 2004-01-14 2004-02-18 Celltech R&D Ltd Novel compounds

Also Published As

Publication number Publication date
US8071780B2 (en) 2011-12-06
EP1636186A1 (en) 2006-03-22
AU2004247469A1 (en) 2004-12-23
IL172542A (en) 2011-07-31
GB0313678D0 (en) 2003-07-16
CN1805933A (zh) 2006-07-19
CA2528323A1 (en) 2004-12-23
BRPI0411308A8 (pt) 2017-12-26
JP4780785B2 (ja) 2011-09-28
WO2004111002A1 (en) 2004-12-23
CN100422149C (zh) 2008-10-01
AU2004247469B2 (en) 2009-11-19
BRPI0411308A (pt) 2006-07-11
US20070112028A1 (en) 2007-05-17
JP2006527253A (ja) 2006-11-30
IL172542A0 (en) 2006-04-10

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Effective date: 20200831