AU2013320636A1 - Hydropyrrolopyrrole derivatives for use as fatty acid synthase inhibitors - Google Patents

Hydropyrrolopyrrole derivatives for use as fatty acid synthase inhibitors Download PDF

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Publication number
AU2013320636A1
AU2013320636A1 AU2013320636A AU2013320636A AU2013320636A1 AU 2013320636 A1 AU2013320636 A1 AU 2013320636A1 AU 2013320636 A AU2013320636 A AU 2013320636A AU 2013320636 A AU2013320636 A AU 2013320636A AU 2013320636 A1 AU2013320636 A1 AU 2013320636A1
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AU
Australia
Prior art keywords
denotes
formula
atoms
pharmaceutically acceptable
tautomers
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
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AU2013320636A
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English (en)
Inventor
Frank CZAUDERNA
Brigitta Leuthner
Wolfgang Staehle
Christos Tsaklakidis
Ansgar Wegener
Dirk Wienke
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Merck Patent GmbH
Original Assignee
Merck Patent GmbH
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 Merck Patent GmbH filed Critical Merck Patent GmbH
Publication of AU2013320636A1 publication Critical patent/AU2013320636A1/en
Abandoned legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • 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
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/407Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/472Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pain & Pain Management (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Cardiology (AREA)
  • Rheumatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
AU2013320636A 2012-09-24 2013-08-30 Hydropyrrolopyrrole derivatives for use as fatty acid synthase inhibitors Abandoned AU2013320636A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP12006668 2012-09-24
EP12006668.3 2012-09-24
PCT/EP2013/002606 WO2014044356A1 (en) 2012-09-24 2013-08-30 Hydropyrrolopyrrole derivatives for use as fatty acid synthase inhibitors

Publications (1)

Publication Number Publication Date
AU2013320636A1 true AU2013320636A1 (en) 2015-05-07

Family

ID=47088611

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2013320636A Abandoned AU2013320636A1 (en) 2012-09-24 2013-08-30 Hydropyrrolopyrrole derivatives for use as fatty acid synthase inhibitors

Country Status (16)

Country Link
US (1) US9416133B2 (https=)
EP (1) EP2897958B1 (https=)
JP (1) JP6259460B2 (https=)
KR (1) KR20150061644A (https=)
CN (1) CN104640866B (https=)
AR (1) AR092211A1 (https=)
AU (1) AU2013320636A1 (https=)
BR (1) BR112015005862A2 (https=)
CA (1) CA2885673A1 (https=)
ES (1) ES2608040T3 (https=)
HK (1) HK1210470A1 (https=)
IL (1) IL237839A0 (https=)
MX (1) MX2015003542A (https=)
RU (1) RU2015115278A (https=)
SG (1) SG11201502014XA (https=)
WO (1) WO2014044356A1 (https=)

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WO2013132253A1 (en) 2012-03-07 2013-09-12 Institute Of Cancer Research: Royal Cancer Hospital (The) 3-aryl-5-substituted-isoquinolin-1-one compounds and their therapeutic use
AR095079A1 (es) 2013-03-12 2015-09-16 Hoffmann La Roche Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo
ES2753386T3 (es) 2013-03-13 2020-04-08 Forma Therapeutics Inc Derivados de 2-hidroxi-1-{4-[(4-fenil)fenil]carbonil}piperazin-1-il}etano-1-ona y compuestos relacionados como inhibidores de sintasa de ácido graso (FASN) para el tratamiento del cáncer
EP3044221B1 (en) 2013-09-11 2018-02-21 Institute of Cancer Research: Royal Cancer Hospital (The) 3-aryl-5-substituted-isoquinolin-1-one compounds and their therapeutic use
DK3074400T3 (en) 2013-11-26 2018-01-15 Hoffmann La Roche Octahydro-cyclobuta [1,2-c; 3,4-c '] dipyrrole derivatives as autotaxin inhibitors
CA2937616A1 (en) 2014-03-26 2015-10-01 F. Hoffmann-La Roche Ag Bicyclic compounds as autotaxin (atx) and lysophosphatidic acid (lpa) production inhibitors
KR20180026459A (ko) 2015-06-18 2018-03-12 세파론, 인코포레이티드 1,4-치환된 피페리딘 유도체
WO2016205590A1 (en) 2015-06-18 2016-12-22 Cephalon, Inc. Substituted 4-benzyl and 4-benzoyl piperidine derivatives
CA2992889A1 (en) 2015-09-04 2017-03-09 F. Hoffmann-La Roche Ag Phenoxymethyl derivatives
WO2017050732A1 (en) 2015-09-24 2017-03-30 F. Hoffmann-La Roche Ag Bicyclic compounds as atx inhibitors
JP6876685B2 (ja) 2015-09-24 2021-05-26 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft Atx阻害剤としての二環式化合物
BR112017026682A2 (pt) * 2015-09-24 2018-08-14 Hoffmann La Roche novos compostos bicíclicos como inibidores de dupla ação de atx/ca
WO2017156350A1 (en) 2016-03-09 2017-09-14 K-Gen, Inc. Methods of cancer treatment
RU2019132254A (ru) 2017-03-16 2021-04-16 Ф. Хоффманн-Ля Рош Аг Гетероциклические соединения, пригодные в качестве дуальных ингибиторов atx/ca
JP7090099B2 (ja) 2017-03-16 2022-06-23 エフ.ホフマン-ラ ロシュ アーゲー Atxインヒビターとしての新規二環式化合物
LT3483164T (lt) 2017-03-20 2020-05-11 Forma Therapeutics, Inc. Pirolpirolo kompozicijos kaip piruvato kinazės (pkr) aktyvatoriai
EP3852791B1 (en) 2018-09-19 2024-07-03 Novo Nordisk Health Care AG Activating pyruvate kinase r
EP3853206B1 (en) 2018-09-19 2024-04-10 Novo Nordisk Health Care AG Treating sickle cell disease with a pyruvate kinase r activating compound
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
HRP20251148T1 (hr) 2019-09-19 2025-11-21 Novo Nordisk Health Care Ag Pripravci koji aktiviraju piruvat-kinazu r (pkr)
US12128035B2 (en) 2021-03-19 2024-10-29 Novo Nordisk Health Care Ag Activating pyruvate kinase R

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2008136756A (ru) * 2006-02-15 2010-03-20 Ф.Хоффманн-Ля Рош Аг (Ch) Гетеробициклические противовирусные соединения
EP2010172B1 (en) * 2006-04-07 2012-08-29 Janssen Pharmaceutica N.V. Indoles and benzoimidazoles as modulators of the histamine h4 receptor
WO2008059214A1 (en) * 2006-11-13 2008-05-22 Astrazeneca Ab Bisamlde derivatives and use thereof as fatty acid synthase inhibitors
CA2679735A1 (en) * 2007-03-01 2008-09-12 Janssen Pharmaceutica N.V. Tetrahydroisoquinoline compounds as modulators of the histamine h3 receptor
EP2170064A4 (en) * 2007-06-22 2010-08-04 Merck Sharp & Dohme 6,5-pyrrolopiperidine tachykinin receptor antagonists
WO2011048018A1 (en) 2009-10-19 2011-04-28 Boehringer Ingelheim International Gmbh Cyclopentanecarboxamide derivatives, medicaments containing such compounds and their use
WO2011056635A1 (en) 2009-10-27 2011-05-12 Glaxosmithkline Llc Benzimidazoles as fatty acid synthase inhibitors
US8633183B2 (en) * 2010-01-26 2014-01-21 Boehringer Ingelheim International Gmbh 5-alkynyl-pyrimidines
WO2012064642A1 (en) 2010-11-08 2012-05-18 Glaxosmithkline Llc Fatty acid synthase inhibitors
EP3190108B1 (en) * 2011-03-08 2021-05-19 Sagimet Biosciences Inc. Heterocyclic modulators of lipid synthesis
WO2013028445A1 (en) 2011-08-19 2013-02-28 Glaxosmithkline Llc Fatty acid synthase inhibitors

Also Published As

Publication number Publication date
US9416133B2 (en) 2016-08-16
CN104640866B (zh) 2017-06-06
HK1210470A1 (en) 2016-04-22
KR20150061644A (ko) 2015-06-04
WO2014044356A1 (en) 2014-03-27
CN104640866A (zh) 2015-05-20
MX2015003542A (es) 2015-07-17
BR112015005862A2 (pt) 2017-07-04
AR092211A1 (es) 2015-04-08
SG11201502014XA (en) 2015-04-29
JP6259460B2 (ja) 2018-01-10
ES2608040T3 (es) 2017-04-05
RU2015115278A (ru) 2016-11-20
EP2897958A1 (en) 2015-07-29
EP2897958B1 (en) 2016-09-21
CA2885673A1 (en) 2014-03-27
US20150252046A1 (en) 2015-09-10
IL237839A0 (en) 2015-05-31
JP2015529229A (ja) 2015-10-05

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MK4 Application lapsed section 142(2)(d) - no continuation fee paid for the application