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WO2002009651A3 - Fatty acid synthase inhibitors - Google Patents

Fatty acid synthase inhibitors Download PDF

Info

Publication number
WO2002009651A3
WO2002009651A3 PCT/US2001/024366 US0124366W WO0209651A3 WO 2002009651 A3 WO2002009651 A3 WO 2002009651A3 US 0124366 W US0124366 W US 0124366W WO 0209651 A3 WO0209651 A3 WO 0209651A3
Authority
WO
WIPO (PCT)
Prior art keywords
fatty acid
acid synthase
synthase inhibitors
inhibitors
compounds
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/US2001/024366
Other languages
French (fr)
Other versions
WO2002009651A2 (en
Inventor
Siegfried B Christensen Iv
Robert A Daines
Jinhwa Lee
Jian-Ning Xiang
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.)
SmithKline Beecham Corp
Original Assignee
SmithKline Beecham 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 SmithKline Beecham Corp filed Critical SmithKline Beecham Corp
Priority to AU2001284705A priority Critical patent/AU2001284705A1/en
Priority to JP2002515206A priority patent/JP2004505030A/en
Priority to EP01963783A priority patent/EP1322331A2/en
Publication of WO2002009651A2 publication Critical patent/WO2002009651A2/en
Publication of WO2002009651A3 publication Critical patent/WO2002009651A3/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D257/00—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms
    • C07D257/02—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D257/04—Five-membered rings
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C323/00—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
    • C07C323/10—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and singly-bound oxygen atoms bound to the same carbon skeleton
    • C07C323/18—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and singly-bound oxygen atoms bound to the same carbon skeleton having the sulfur atom of at least one of the thio groups bound to a carbon atom of a six-membered aromatic ring of the carbon skeleton
    • C07C323/20—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and singly-bound oxygen atoms bound to the same carbon skeleton having the sulfur atom of at least one of the thio groups bound to a carbon atom of a six-membered aromatic ring of the carbon skeleton with singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C323/00—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
    • C07C323/50—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton
    • C07C323/51—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C323/56—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton containing six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C323/00—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
    • C07C323/50—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton
    • C07C323/51—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C323/60—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton with the carbon atom of at least one of the carboxyl groups bound to nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00—Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/40—Unsaturated compounds
    • C07C59/58—Unsaturated compounds containing ether groups, groups, groups, or groups
    • C07C59/64—Unsaturated compounds containing ether groups, groups, groups, or groups containing six-membered aromatic rings
    • C07C59/66—Unsaturated compounds containing ether groups, groups, groups, or groups containing six-membered aromatic rings the non-carboxylic part of the ether containing six-membered aromatic rings
    • C07C59/68—Unsaturated compounds containing ether groups, groups, groups, or groups containing six-membered aromatic rings the non-carboxylic part of the ether containing six-membered aromatic rings the oxygen atom of the ether group being bound to a non-condensed six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D257/00—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms
    • C07D257/02—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D257/04—Five-membered rings
    • C07D257/06—Five-membered rings with nitrogen atoms directly attached to the ring carbon atom
    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/02—Systems containing only non-condensed rings with a three-membered ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/12—Systems containing only non-condensed rings with a six-membered ring
    • C07C2601/14—The ring being saturated

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Heterocyclic Compounds Containing Sulfur Atoms (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

This invention relates to the use of compounds as inhibitors of the fatty acid synthase FabH.
PCT/US2001/024366 2000-08-02 2001-08-02 Fatty acid synthase inhibitors Ceased WO2002009651A2 (en)

Priority Applications (3)

Application Number Priority Date Filing Date Title
AU2001284705A AU2001284705A1 (en) 2000-08-02 2001-08-02 Fatty acid synthase inhibitors
JP2002515206A JP2004505030A (en) 2000-08-02 2001-08-02 Fatty acid synthase inhibitors
EP01963783A EP1322331A2 (en) 2000-08-02 2001-08-02 Fatty acid synthase inhibitors

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US22268300P 2000-08-02 2000-08-02
US60/222,683 2000-08-02

Publications (2)

Publication Number Publication Date
WO2002009651A2 WO2002009651A2 (en) 2002-02-07
WO2002009651A3 true WO2002009651A3 (en) 2002-03-28

Family

ID=22833247

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2001/024366 Ceased WO2002009651A2 (en) 2000-08-02 2001-08-02 Fatty acid synthase inhibitors

Country Status (4)

Country Link
EP (1) EP1322331A2 (en)
JP (1) JP2004505030A (en)
AU (1) AU2001284705A1 (en)
WO (1) WO2002009651A2 (en)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ME03564B (en) 2013-03-13 2020-07-20 Forma Therapeutics Inc 2-hydroxy-1-{4-[(4-phenylphenyl)carbonyl]piperazin-1-yl}ethan-1-one derivatives and related compounds as fatty acid synthase (fasn) inhibitors for the treatment of cancer
TWI767148B (en) 2018-10-10 2022-06-11 美商弗瑪治療公司 Inhibiting fatty acid synthase (fasn)
CN113382633A (en) 2018-10-29 2021-09-10 福马治疗股份有限公司 Solid forms of (4- (2-fluoro-4- (1-methyl-1H-benzo [ d ] imidazol-5-yl) benzoyl) piperazin-1-yl) (1-hydroxycyclopropyl) methanone

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES451822A1 (en) * 1975-09-25 1977-12-16 American Cyanamid Co PROCEDURE TO PREPARE HYPOLIPEMIC COMPOUNDS.
US4125732A (en) * 1977-05-06 1978-11-14 American Cyanamid Company 2-Aryloxy-2-(phenoxyalkoxy)phenyl acetic acid and esters
US4168385A (en) * 1975-09-25 1979-09-18 American Cyanamid Company Hypolipemic phenylacetic acid derivatives
US4496738A (en) * 1978-10-23 1985-01-29 Basf Aktiengesellschaft Process for preparing 1,2,4-triazole derivatives
JPS63307837A (en) * 1986-09-08 1988-12-15 Daicel Chem Ind Ltd Optical active compound
WO2000034254A1 (en) * 1998-12-04 2000-06-15 Astrazeneca Ab Novel compounds

Patent Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES451822A1 (en) * 1975-09-25 1977-12-16 American Cyanamid Co PROCEDURE TO PREPARE HYPOLIPEMIC COMPOUNDS.
US4125729A (en) * 1975-09-25 1978-11-14 American Cyanamid Company Hypolipemic α-aryloxy para substituted phenyl acetic acid compounds
US4168385A (en) * 1975-09-25 1979-09-18 American Cyanamid Company Hypolipemic phenylacetic acid derivatives
US4125732A (en) * 1977-05-06 1978-11-14 American Cyanamid Company 2-Aryloxy-2-(phenoxyalkoxy)phenyl acetic acid and esters
US4496738A (en) * 1978-10-23 1985-01-29 Basf Aktiengesellschaft Process for preparing 1,2,4-triazole derivatives
JPS63307837A (en) * 1986-09-08 1988-12-15 Daicel Chem Ind Ltd Optical active compound
JP2562606B2 (en) * 1986-09-08 1996-12-11 ダイセル化学工業株式会社 Optically active compound
WO2000034254A1 (en) * 1998-12-04 2000-06-15 Astrazeneca Ab Novel compounds

Also Published As

Publication number Publication date
AU2001284705A1 (en) 2002-02-13
WO2002009651A2 (en) 2002-02-07
EP1322331A2 (en) 2003-07-02
JP2004505030A (en) 2004-02-19

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