SG183260A1 - Triazolones as fatty acid synthase inhibitors - Google Patents

Triazolones as fatty acid synthase inhibitors Download PDF

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Publication number
SG183260A1
SG183260A1 SG2012059291A SG2012059291A SG183260A1 SG 183260 A1 SG183260 A1 SG 183260A1 SG 2012059291 A SG2012059291 A SG 2012059291A SG 2012059291 A SG2012059291 A SG 2012059291A SG 183260 A1 SG183260 A1 SG 183260A1
Authority
SG
Singapore
Prior art keywords
dihydro
cyclopropylcarbonyl
triazol
mmol
methyl
Prior art date
Application number
SG2012059291A
Other languages
English (en)
Inventor
Nicholas D Adams
Christopher Joseph Aquino
Amita M Chaudhari
Jonathan M Ghergurovich
Terence John Kiesow
Cynthia A Parrish
Alexander Joseph Reif
Kenneth Wiggall
Original Assignee
Glaxosmithkline Llc
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 Glaxosmithkline Llc filed Critical Glaxosmithkline Llc
Publication of SG183260A1 publication Critical patent/SG183260A1/en

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D407/00Heterocyclic 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
    • C07D407/14Heterocyclic 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 three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/397Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41961,2,4-Triazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
SG2012059291A 2010-02-22 2011-02-22 Triazolones as fatty acid synthase inhibitors SG183260A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US30670910P 2010-02-22 2010-02-22
US35758710P 2010-06-23 2010-06-23
PCT/US2011/025661 WO2011103546A1 (en) 2010-02-22 2011-02-22 Triazolones as fatty acid synthase inhibitors

Publications (1)

Publication Number Publication Date
SG183260A1 true SG183260A1 (en) 2012-09-27

Family

ID=44483349

Family Applications (1)

Application Number Title Priority Date Filing Date
SG2012059291A SG183260A1 (en) 2010-02-22 2011-02-22 Triazolones as fatty acid synthase inhibitors

Country Status (13)

Country Link
US (2) US8802864B2 (enExample)
EP (1) EP2538787B1 (enExample)
JP (1) JP5805672B2 (enExample)
KR (1) KR20120133386A (enExample)
CN (1) CN102858175A (enExample)
AU (1) AU2011217809A1 (enExample)
BR (1) BR112012020976A2 (enExample)
CA (1) CA2790692A1 (enExample)
EA (1) EA201290822A1 (enExample)
ES (1) ES2509951T3 (enExample)
MX (1) MX2012009720A (enExample)
SG (1) SG183260A1 (enExample)
WO (1) WO2011103546A1 (enExample)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2011217809A1 (en) * 2010-02-22 2012-09-06 Glaxosmithkline Llc Triazolones as fatty acid synthase inhibitors
EP2822931B1 (en) * 2012-03-09 2017-05-03 Inception 2, Inc. Triazolone compounds and uses thereof
JP6404230B2 (ja) 2012-12-20 2018-10-10 インセプション 2、 インコーポレイテッド トリアゾロン化合物およびその使用
ES2651331T3 (es) * 2013-01-10 2018-01-25 Glaxosmithkline Intellectual Property (No. 2) Limited Inhibidores de la sintasa de ácidos grasos
CN112521369A (zh) 2013-03-13 2021-03-19 福马治疗股份有限公司 用于抑制fasn的化合物及组合物
UY35728A (es) 2013-09-05 2015-04-30 Dow Agrosciences Llc ?métodos para producir arenos borilados?.
CA2921420A1 (en) 2013-09-06 2015-03-12 Inception 2, Inc. Triazolone compounds and uses thereof
CA2934257C (en) 2013-12-17 2022-06-07 Janssen Pharmaceutica Nv Imidazolin-5-one derivative useful as fasn inhibitors for the treatment of cancer
TW201625354A (zh) 2014-06-16 2016-07-16 陶氏農業科學公司 用於製備氧硼基化芳烴之方法
CN104876917B (zh) * 2015-06-16 2017-09-19 上海皓元医药股份有限公司 用作脂肪酸合成酶抑制剂的三唑酮的合成方法
EP3310773B1 (en) 2015-06-18 2020-12-02 89Bio Ltd. Substituted 4-benzyl and 4-benzoyl piperidine derivatives
CN107847765B (zh) 2015-06-18 2021-05-04 89生物有限公司 1,4-取代的哌啶衍生物
TW201722957A (zh) * 2015-09-15 2017-07-01 葛蘭素史克智慧財產(第二)有限公司 化學化合物
TWI767148B (zh) 2018-10-10 2022-06-11 美商弗瑪治療公司 抑制脂肪酸合成酶(fasn)
WO2020092395A1 (en) 2018-10-29 2020-05-07 Forma Therapeutics, Inc. SOLID FORMS OF (4-(2-FLUORO-4-(1-METHYL-1 H-BENZO[d]IMIDAZOL-5-YL)BENZOYL) PIPERAZIN-1-YL)(1-HYDROXYCYCLOPROPYL)METHANONE
CN114539193B (zh) * 2022-01-20 2024-08-06 安徽普利药业有限公司 一种盐酸胺碘酮中间体的制备方法

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5728834A (en) * 1996-11-14 1998-03-17 Wyckoff Chemical Company, Inc. Process for preparation of 4-aryl-1,2,4-triazol-3-ones
KR20050100615A (ko) * 2003-01-14 2005-10-19 싸이토키네틱스, 인코포레이티드 화합물, 조성물 및 방법
SE0400850D0 (sv) * 2004-03-30 2004-03-31 Astrazeneca Ab Novel Compounds
DK1784396T3 (da) * 2004-08-26 2011-02-14 Pfizer Pyrazol-substituerede aminoheteroaryl-forbindelser som proteinkinase-inhibitorer
WO2007056170A2 (en) * 2005-11-02 2007-05-18 Bayer Healthcare Ag Pyrrolo[2,1-f] [1,2,4] triazin-4-ylamines igf-1r kinase inhibitors for the treatment of cancer and other hyperproliferative diseases
US8236792B2 (en) 2008-05-23 2012-08-07 Janssen Pharmaceutica Nv Substituted pyrrolidine amides as modulators of the histamine H3 receptor
AU2011217809A1 (en) * 2010-02-22 2012-09-06 Glaxosmithkline Llc Triazolones as fatty acid synthase inhibitors

Also Published As

Publication number Publication date
US8802864B2 (en) 2014-08-12
CA2790692A1 (en) 2011-08-25
AU2011217809A1 (en) 2012-09-06
EP2538787B1 (en) 2014-07-16
EA201290822A1 (ru) 2013-03-29
JP2013520443A (ja) 2013-06-06
EP2538787A4 (en) 2013-07-17
KR20120133386A (ko) 2012-12-10
US20140100213A1 (en) 2014-04-10
BR112012020976A2 (pt) 2017-05-09
WO2011103546A1 (en) 2011-08-25
ES2509951T3 (es) 2014-10-20
CN102858175A (zh) 2013-01-02
US20120316151A1 (en) 2012-12-13
US9340529B2 (en) 2016-05-17
EP2538787A1 (en) 2013-01-02
JP5805672B2 (ja) 2015-11-04
MX2012009720A (es) 2012-10-09

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