WO2008150486A3 - 2-acylaminopropoanol-type glucosylceramide synthase inhibitors - Google Patents

2-acylaminopropoanol-type glucosylceramide synthase inhibitors Download PDF

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Publication number
WO2008150486A3
WO2008150486A3 PCT/US2008/006906 US2008006906W WO2008150486A3 WO 2008150486 A3 WO2008150486 A3 WO 2008150486A3 US 2008006906 W US2008006906 W US 2008006906W WO 2008150486 A3 WO2008150486 A3 WO 2008150486A3
Authority
WO
WIPO (PCT)
Prior art keywords
subject
pharmaceutically acceptable
acceptable salt
structural formula
compound represented
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
PCT/US2008/006906
Other languages
French (fr)
Other versions
WO2008150486A2 (en
Inventor
Craig Siegel
Cecilia M Bastos
David J Harris
Angeles Dios
Edward Lee
Richard Silva
Lisa M Cuff
Mikaela Levine
Cassandra Celatka
Frederic Vinick
Thomas Jozefiak
Yibin Xiang
John Kane
Junkai Liao
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.)
Genzyme Corp
Original Assignee
Genzyme Corp
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 Genzyme Corp filed Critical Genzyme Corp
Priority to EP13154955.2A priority Critical patent/EP2594563B1/en
Priority to EP08768008.8A priority patent/EP2167485B1/en
Priority to US12/601,871 priority patent/US8304447B2/en
Priority to EP13154970.1A priority patent/EP2594565B1/en
Priority to HK10105161.0A priority patent/HK1138282B/en
Publication of WO2008150486A2 publication Critical patent/WO2008150486A2/en
Publication of WO2008150486A3 publication Critical patent/WO2008150486A3/en
Anticipated expiration legal-status Critical
Priority to US13/595,349 priority patent/US8940776B2/en
Priority to US14/571,922 priority patent/US9745294B2/en
Priority to US15/649,128 priority patent/US20180093981A1/en
Ceased legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/12—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms
    • C07D295/125—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D319/00—Heterocyclic compounds containing six-membered rings having two oxygen atoms as the only ring hetero atoms
    • C07D319/10—1,4-Dioxanes; Hydrogenated 1,4-dioxanes
    • C07D319/14—1,4-Dioxanes; Hydrogenated 1,4-dioxanes condensed with carbocyclic rings or ring systems
    • C07D319/16—1,4-Dioxanes; Hydrogenated 1,4-dioxanes condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C07D319/18—Ethylenedioxybenzenes, not substituted on the hetero ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
    • C07D407/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D411/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms
    • C07D411/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D411/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Diabetes (AREA)
  • General Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

A compound is represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating a subject in need thereof comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. The subject has type 2 diabetes; renal hypertrophy or hyperplasia associated with diabetic nephropathy; Tay-Sachs; Gaucher's; or Fabry's disease. Methods of decreasing plasma TNF-α, lowering blood glucose levels, decreasing glycated hemoglobin levels, inhibiting glucosylceramide synthase, and lowering glycosphingolipid concentrations in a subject in need thereof respectively comprise administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.
PCT/US2008/006906 2007-05-31 2008-05-30 2-acylaminopropoanol-type glucosylceramide synthase inhibitors Ceased WO2008150486A2 (en)

Priority Applications (8)

Application Number Priority Date Filing Date Title
EP13154955.2A EP2594563B1 (en) 2007-05-31 2008-05-30 2-acylaminopropanol-type glucosylceramide synthase inhibitors
EP08768008.8A EP2167485B1 (en) 2007-05-31 2008-05-30 2-acylaminopropoanol-type glucosylceramide synthase inhibitors
US12/601,871 US8304447B2 (en) 2007-05-31 2008-05-30 2-acylaminopropoanol-type glucosylceramide synthase inhibitors
EP13154970.1A EP2594565B1 (en) 2007-05-31 2008-05-30 2-acylaminopropanol-type glucosylceramide synthase inhibitors
HK10105161.0A HK1138282B (en) 2007-05-31 2008-05-30 2-acylaminopropoanol-type glucosylceramide synthase inhibitors
US13/595,349 US8940776B2 (en) 2007-05-31 2012-08-27 2-acylaminopropoanol-type glucosylceramide synthase inhibitors
US14/571,922 US9745294B2 (en) 2007-05-31 2014-12-16 2-acylaminopropoanol-type glucosylceramide synthase inhibitors
US15/649,128 US20180093981A1 (en) 2007-05-31 2017-07-13 2-Acylaminopropoanol-Type Glucosylceramide Synthase Inhibitors

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US93237007P 2007-05-31 2007-05-31
US60/932,370 2007-05-31
US99784607P 2007-10-05 2007-10-05
US60/997,846 2007-10-05

Related Child Applications (2)

Application Number Title Priority Date Filing Date
US12/601,871 A-371-Of-International US8304447B2 (en) 2007-05-31 2008-05-30 2-acylaminopropoanol-type glucosylceramide synthase inhibitors
US13/595,349 Continuation US8940776B2 (en) 2007-05-31 2012-08-27 2-acylaminopropoanol-type glucosylceramide synthase inhibitors

Publications (2)

Publication Number Publication Date
WO2008150486A2 WO2008150486A2 (en) 2008-12-11
WO2008150486A3 true WO2008150486A3 (en) 2009-02-05

Family

ID=39730765

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2008/006906 Ceased WO2008150486A2 (en) 2007-05-31 2008-05-30 2-acylaminopropoanol-type glucosylceramide synthase inhibitors

Country Status (4)

Country Link
US (4) US8304447B2 (en)
EP (5) EP2594562B1 (en)
AR (1) AR066817A1 (en)
WO (1) WO2008150486A2 (en)

Cited By (2)

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US9150505B2 (en) 2010-03-04 2015-10-06 Ajinomoto Co., Inc. Prophylactic or therapeutic agent for diabetes or obesity
US11014935B2 (en) 2012-08-23 2021-05-25 Janssen Biopharma, Inc. Compounds for the treatment of paramyxovirus viral infections

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JP2008519840A (en) 2004-11-10 2008-06-12 ジェンザイム・コーポレイション How to treat diabetes
WO2007134086A2 (en) 2006-05-09 2007-11-22 Genzyme Corporation Methods of treating fatty liver disease comprising inhibiting glucosphingolipid synthesis
EP2594562B1 (en) 2007-05-31 2016-07-20 Genzyme Corporation 2-acylaminopropanol-type glucosylceramide synthase inhibitors
KR101640263B1 (en) * 2007-10-05 2016-07-15 젠자임 코포레이션 Method of treating polycystic kidney diseases with ceramide derivatives
WO2009117150A2 (en) * 2008-03-20 2009-09-24 Genzyme Corporation Method of treating lupus with ceramide derivatives
JP2011529500A (en) 2008-07-28 2011-12-08 ジェンザイム コーポレーション Glucosylceramide synthase inhibition for the treatment of collapsing glomerulopathy and other glomerular diseases
US8309593B2 (en) 2008-10-03 2012-11-13 Genzyme Corporation 2-acylaminopropoanol-type glucosylceramide synthase inhibitors
WO2010091104A1 (en) * 2009-02-06 2010-08-12 Exelixis, Inc. Glucosylceramide synthase inhibitors
WO2010091164A1 (en) * 2009-02-06 2010-08-12 Exelixis, Inc. Inhibitors of glucosylceramide synthase
SG10201407881WA (en) * 2009-11-27 2015-01-29 Genzyme Corp An amorphous and a crystalline form of genz 112638 hemitartrate as inhibitor of glucosylceramide synthase
CN102838505B (en) 2011-06-24 2016-02-17 上海医药工业研究院 Amides, its preparation method and application
EP2567959B1 (en) 2011-09-12 2014-04-16 Sanofi 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
WO2013059119A1 (en) * 2011-10-17 2013-04-25 The Regents Of The University Of Michigan Glucosylceramide synthase inhibitors and therapeutic methods using the same
PH12021550330A1 (en) * 2013-08-21 2022-09-28 Janssen Biopharma Inc Antiviral compounds
AU2014321397C1 (en) * 2013-09-20 2019-08-01 Biomarin Pharmaceutical Inc. Glucosylceramide synthase inhibitors for the treatment of diseases
CN105849102B (en) * 2013-10-29 2020-10-16 生物马林药物股份有限公司 N- (1-hydroxy-3 (pyrrolidinyl) propan-2-yl) pyrrolidine-3-carboxamide derivatives as glucosylceramide synthase inhibitors
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WO2016126572A2 (en) 2015-02-02 2016-08-11 The Regents Of The University Of Michigan Glucosylceramide synthase inhibitors and therapeutic methods using the same
EP3268355B1 (en) * 2015-03-11 2019-06-12 BioMarin Pharmaceutical Inc. Glucosylceramide synthase inhibitors for the treatment of diseases
JP6895963B2 (en) 2015-11-18 2021-06-30 ジェンザイム・コーポレーション Biomarkers for polycystic kidney disease and their use
JP6940515B2 (en) 2016-03-25 2021-09-29 ジェンザイム・コーポレーション Biomarkers of proteinosis and their use
US20200339587A1 (en) 2017-12-21 2020-10-29 Lysosomal Therapeutics Inc. Crystalline substituted cyclohexyl pyrazolo[1,5-a]pyrimidinyl carboxamide compound and therapeutic uses thereof
WO2020193746A1 (en) 2019-03-28 2020-10-01 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for predicting the survival of patients suffering from melanoma
US11220479B2 (en) 2019-10-23 2022-01-11 The Regents Of The University Of Michigan Glucosylceramide synthase inhibitors and therapeutic methods using the same
US20230002380A1 (en) 2019-11-15 2023-01-05 Yuhan Corporation Novel compounds having inhibitory activity against glucosylceramide synthase or pharmaceutically acceptable salt thereof, processes for preparing the same, and pharmaceutical compositions comprising the same
BR112022009409A2 (en) 2019-11-15 2022-08-09 Yuhan Corp NEW DERIVATIVES THAT HAVE 2,3-DIHYDRO-1H-INDENE OR 2,3-DIHYDROBENZOFURAN OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF AND PHARMACEUTICAL COMPOSITIONS COMPRISING THEM
EP4142878B1 (en) 2020-04-28 2024-06-26 The Regents of The University of Michigan Pyridine inhibitors of glucosylceramide synthase and therapeutic methods using the same

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