CA2790692A1 - Triazolones as fatty acid synthase inhibitors - Google Patents

Triazolones as fatty acid synthase inhibitors Download PDF

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Publication number
CA2790692A1
CA2790692A1 CA2790692A CA2790692A CA2790692A1 CA 2790692 A1 CA2790692 A1 CA 2790692A1 CA 2790692 A CA2790692 A CA 2790692A CA 2790692 A CA2790692 A CA 2790692A CA 2790692 A1 CA2790692 A1 CA 2790692A1
Authority
CA
Canada
Prior art keywords
dihydro
methyl
cyclopropylcarbonyl
triazol
pyrrolidinyl
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.)
Abandoned
Application number
CA2790692A
Other languages
English (en)
French (fr)
Inventor
Nicholas D. Adams
Christopher Joseph Aquino
Amita M. Chaudhari
Jonathan M. Ghergurovich
Terence John Kiesow
Cynthia A. Parrish
Alexander Joseph Reif
Kenneth Wiggall
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.)
GlaxoSmithKline LLC
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 CA2790692A1 publication Critical patent/CA2790692A1/en
Abandoned legal-status Critical Current

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic 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
    • 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
    • C07D407/14—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 three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic 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
    • A61K31/4196—1,2,4-Triazoles
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/06—Heterocyclic 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
    • 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
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CA2790692A 2010-02-22 2011-02-22 Triazolones as fatty acid synthase inhibitors Abandoned CA2790692A1 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US30670910P 2010-02-22 2010-02-22
US61/306,709 2010-02-22
US35758710P 2010-06-23 2010-06-23
US61/357,587 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
CA2790692A1 true CA2790692A1 (en) 2011-08-25

Family

ID=44483349

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2790692A Abandoned CA2790692A1 (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
CN102858175A (zh) * 2010-02-22 2013-01-02 葛兰素史密斯克莱有限责任公司 作为脂肪酸合成酶抑制剂的三唑酮
WO2013134562A1 (en) * 2012-03-09 2013-09-12 Inception 2, Inc. Triazolone compounds and uses thereof
DK2935228T3 (en) 2012-12-20 2017-10-30 Inception 2 Inc TRIAZOLONE COMPOUNDS AND APPLICATIONS THEREOF
WO2014108858A1 (en) 2013-01-10 2014-07-17 Glaxosmithkline Intellectual Property (No.2) Limited Fatty acid synthase inhibitors
KR102194745B1 (ko) 2013-03-13 2020-12-24 포르마 세라퓨틱스 인크. Ｆａｓｎ 억제용 신규 화합물 및 조성물
JP6434522B2 (ja) 2013-09-05 2018-12-05 ダウ アグロサイエンシィズ エルエルシー ホウ素化アレーンを生成する方法
CA2921420A1 (en) 2013-09-06 2015-03-12 Inception 2, Inc. Triazolone compounds and uses thereof
EP3083600B1 (en) 2013-12-17 2018-09-26 Janssen Pharmaceutica NV Imidazolin-5-one derivatives 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
US10919875B2 (en) 2015-06-18 2021-02-16 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)
US10793554B2 (en) 2018-10-29 2020-10-06 Forma Therapeutics, Inc. Solid forms of 4-(2-fluoro-4-(1-methyl-1H-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
NZ540878A (en) * 2003-01-14 2008-06-30 Cytokinetics Inc Compounds, compositions and methods
SE0400850D0 (sv) * 2004-03-30 2004-03-31 Astrazeneca Ab Novel Compounds
ATE492544T1 (de) * 2004-08-26 2011-01-15 Pfizer Pyrazol-substituierte aminoheteroarylverbindungen als proteinkinasehemmer
EP1945222B1 (en) * 2005-11-02 2012-12-26 Bayer Pharma Aktiengesellschaft Pyrrolo[2,1-f] [1,2,4]-triazin-4-ylamines as 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
CN102858175A (zh) * 2010-02-22 2013-01-02 葛兰素史密斯克莱有限责任公司 作为脂肪酸合成酶抑制剂的三唑酮

Also Published As

Publication number Publication date
EP2538787B1 (en) 2014-07-16
ES2509951T3 (es) 2014-10-20
WO2011103546A1 (en) 2011-08-25
US20120316151A1 (en) 2012-12-13
EP2538787A1 (en) 2013-01-02
EA201290822A1 (ru) 2013-03-29
EP2538787A4 (en) 2013-07-17
KR20120133386A (ko) 2012-12-10
BR112012020976A2 (pt) 2017-05-09
US9340529B2 (en) 2016-05-17
AU2011217809A1 (en) 2012-09-06
JP2013520443A (ja) 2013-06-06
JP5805672B2 (ja) 2015-11-04
SG183260A1 (en) 2012-09-27
US8802864B2 (en) 2014-08-12
CN102858175A (zh) 2013-01-02
MX2012009720A (es) 2012-10-09
US20140100213A1 (en) 2014-04-10

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Legal Events

Date Code Title Description
FZDE Discontinued

Effective date: 20150224