BR112012020976A2 - triazolonas como inibidores de ácido graxo sintase - Google Patents

triazolonas como inibidores de ácido graxo sintase

Info

Publication number
BR112012020976A2
BR112012020976A2 BR112012020976A BR112012020976A BR112012020976A2 BR 112012020976 A2 BR112012020976 A2 BR 112012020976A2 BR 112012020976 A BR112012020976 A BR 112012020976A BR 112012020976 A BR112012020976 A BR 112012020976A BR 112012020976 A2 BR112012020976 A2 BR 112012020976A2
Authority
BR
Brazil
Prior art keywords
fatty acid
acid synthase
triazolones
synthase inhibitors
relates
Prior art date
Application number
BR112012020976A
Other languages
English (en)
Inventor
Joseph Reif Alexander
M Chaudhari Amita
Joseph Aquino Christopher
A Parrish Cynthia
M Ghergurovich Jonathan
Wiggall Kenneth
D Adams Nicholas
John Kiesow Terence
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 BR112012020976A2 publication Critical patent/BR112012020976A2/pt

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    • 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
    • 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
    • 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)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (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)

Abstract

esta invenção refere-se ao uso de derivados de triazolona para a modulação, notavelmente a inibição da atividade ou função de ácido graxo sintase (fas). adequadamente, a presente invenção refere-se ao udo de triazolonas no tratamento de câncer.
BR112012020976A 2010-02-22 2011-02-22 triazolonas como inibidores de ácido graxo sintase BR112012020976A2 (pt)

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
BR112012020976A2 true BR112012020976A2 (pt) 2017-05-09

Family

ID=44483349

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112012020976A BR112012020976A2 (pt) 2010-02-22 2011-02-22 triazolonas como inibidores de ácido graxo sintase

Country Status (13)

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

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2538787B1 (en) * 2010-02-22 2014-07-16 GlaxoSmithKline LLC Triazolones as fatty acid synthase inhibitors
WO2013134562A1 (en) * 2012-03-09 2013-09-12 Inception 2, Inc. Triazolone compounds and uses thereof
WO2014099503A1 (en) 2012-12-20 2014-06-26 Inception 2, Inc. Triazolone compounds and uses thereof
ES2651331T3 (es) * 2013-01-10 2018-01-25 Glaxosmithkline Intellectual Property (No. 2) Limited Inhibidores de la sintasa de ácidos grasos
RU2737434C2 (ru) 2013-03-13 2020-11-30 Форма Терапьютикс, Инк. Новые соединения и композиции для ингибирования fasn
MX2016002923A (es) 2013-09-05 2017-01-19 Dow Agrosciences Llc Metodos para producir arenos borilados.
PE20160880A1 (es) 2013-09-06 2016-09-22 Inception 2 Inc Compuestos de triazolona y usos de los mismos
JP6617106B2 (ja) * 2013-12-17 2019-12-04 ヤンセン ファーマシューティカ エヌ．ベー． 癌の治療用のｆａｓｎ阻害剤として有用なイミダゾリン−５−オン誘導体
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
CA3014432A1 (en) 2015-06-18 2016-12-22 Cephalon, Inc. Substituted 4-benzyl and 4-benzoyl piperidine derivatives
ES2821049T3 (es) 2015-06-18 2021-04-23 89Bio Ltd Derivados de piperidina 1,4 sustituidos
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
CN114539193A (zh) * 2022-01-20 2022-05-27 海南普利制药股份有限公司 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
JP4613157B2 (ja) * 2003-01-14 2011-01-12 サイトキネティクス・インコーポレーテッド 化合物、組成物および方法
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
US8431695B2 (en) * 2005-11-02 2013-04-30 Bayer Intellectual Property Gmbh 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
EP2538787B1 (en) * 2010-02-22 2014-07-16 GlaxoSmithKline LLC Triazolones as fatty acid synthase inhibitors

Also Published As

Publication number Publication date
JP5805672B2 (ja) 2015-11-04
WO2011103546A1 (en) 2011-08-25
AU2011217809A1 (en) 2012-09-06
ES2509951T3 (es) 2014-10-20
MX2012009720A (es) 2012-10-09
US8802864B2 (en) 2014-08-12
EP2538787A4 (en) 2013-07-17
EP2538787B1 (en) 2014-07-16
SG183260A1 (en) 2012-09-27
EA201290822A1 (ru) 2013-03-29
CN102858175A (zh) 2013-01-02
EP2538787A1 (en) 2013-01-02
US20140100213A1 (en) 2014-04-10
US20120316151A1 (en) 2012-12-13
JP2013520443A (ja) 2013-06-06
CA2790692A1 (en) 2011-08-25
US9340529B2 (en) 2016-05-17
KR20120133386A (ko) 2012-12-10

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B11A Dismissal acc. art.33 of ipl - examination not requested within 36 months of filing
B11Y Definitive dismissal - extension of time limit for request of examination expired [chapter 11.1.1 patent gazette]
B350 Update of information on the portal [chapter 15.35 patent gazette]