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PE20210658A1 - Derivados de triazolopirimidina para usar como inhibidores de ghrelin o-aciltransferasa (goat) - Google Patents

Derivados de triazolopirimidina para usar como inhibidores de ghrelin o-aciltransferasa (goat)

Info

Publication number
PE20210658A1
PE20210658A1 PE2020001164A PE2020001164A PE20210658A1 PE 20210658 A1 PE20210658 A1 PE 20210658A1 PE 2020001164 A PE2020001164 A PE 2020001164A PE 2020001164 A PE2020001164 A PE 2020001164A PE 20210658 A1 PE20210658 A1 PE 20210658A1
Authority
PE
Peru
Prior art keywords
methyl
ghrelin
goat
inhibitors
aciltransferase
Prior art date
Application number
PE2020001164A
Other languages
English (en)
Inventor
Thomas Trieselmann
Cedrickx Godbout
Viktor Vintonyak
Christoph Hoenke
Original Assignee
Boehringer Ingelheim Int
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 Boehringer Ingelheim Int filed Critical Boehringer Ingelheim Int
Publication of PE20210658A1 publication Critical patent/PE20210658A1/es

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Classifications

    • 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
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Diabetes (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Referido a compuestos derivados de triazolopirimidina de formula general (I); en donde R1 es Cl, Br, CN o CH3; R2 es fenilo o piridinilo cada uno de los cuales esta sustituido con un sustituyente R3 que contiene fluor, donde R3 es seleccionado de C1-6-alquilo, 3-7-cicloalquilo, -O-(C1-6-alquilo), entre otros; cada uno sustituido con uno o mas F. Un compuesto seleccionado es 6-{[6-bromo-5-(difluorometoxi)piridin-2-il]metil}-5-metil-[1,2,4]triazolo[1,5-a]pirimidin-7-amina, 6-{[5-bromo-6-(4-fluoro-1H-pirazol-1-il)piridin-2-il]metil}-5-metil-[1,2,4]triazolo[1,5-a]pirimidin-7-amina. Dichos compuestos son inhibidores de la ghrelin O-aciltransferasa (GOAT). Tambien refiere una composicion farmaceutica que comprende dicho compuesto, siendo adecuada para la profilaxis y/o el tratamiento de enfermedades metabolicas, en particular, obesidad.
PE2020001164A 2018-02-02 2019-01-28 Derivados de triazolopirimidina para usar como inhibidores de ghrelin o-aciltransferasa (goat) PE20210658A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP18154831 2018-02-02
PCT/EP2019/051994 WO2019149660A1 (en) 2018-02-02 2019-01-28 Triazolopyrimidine derivatives for use as ghrelin o-acyl transferase (goat) inhibitors

Publications (1)

Publication Number Publication Date
PE20210658A1 true PE20210658A1 (es) 2021-03-31

Family

ID=61157054

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2020001164A PE20210658A1 (es) 2018-02-02 2019-01-28 Derivados de triazolopirimidina para usar como inhibidores de ghrelin o-aciltransferasa (goat)

Country Status (21)

Country Link
US (1) US11583532B2 (es)
EP (1) EP3746443B1 (es)
JP (1) JP7083397B2 (es)
KR (1) KR20200118125A (es)
CN (1) CN111683951B (es)
AU (1) AU2019215710A1 (es)
BR (1) BR112020014436A2 (es)
CA (1) CA3087925A1 (es)
CL (1) CL2020001909A1 (es)
CO (1) CO2020009177A2 (es)
CR (1) CR20200329A (es)
EA (1) EA202091803A1 (es)
EC (1) ECSP20050797A (es)
IL (1) IL276145A (es)
JO (1) JOP20200187A1 (es)
MA (1) MA51774A (es)
MX (1) MX2020007994A (es)
PE (1) PE20210658A1 (es)
PH (1) PH12020551170A1 (es)
SG (1) SG11202006302TA (es)
WO (1) WO2019149660A1 (es)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EA037277B1 (ru) 2016-08-05 2021-03-03 Бёрингер Ингельхайм Интернациональ Гмбх Производные оксадиазолопиридина для применения в качестве ингибиторов грелин-о-ацилтрасферазы (goat)
JOP20200187A1 (ar) 2018-02-02 2020-07-29 Boehringer Ingelheim Int مشتقات ترايازولو بيريميدين للاستخدام كمثبطات جريلين o- أسيل ترانسفيراز (goat)
MX2020008053A (es) 2018-02-02 2020-09-07 Boehringer Ingelheim Int Derivados de oxadiazolopiridina sustituidos con bencilo, (piridin-3-il)metilo o (piridin-4-il)metilo como inhibidores de ghrelin o-aciltransferasa (goat).
CA3173731A1 (en) 2020-02-28 2021-09-02 Kallyope, Inc. Gpr40 agonists
TW202202502A (zh) * 2020-03-26 2022-01-16 美商斯諾皮亞生物科學公司 經同位素標記之曲匹地(trapidil)衍生物
EP4146344A1 (en) 2020-05-04 2023-03-15 Volastra Therapeutics, Inc. Imino sulfanone inhibitors of enpp1
DK4153600T3 (da) 2020-05-22 2024-10-21 Boehringer Ingelheim Int Kontinuerlig fremgangsmåde til fremstilling af alkyl 7-amino-5-methyl-[1,2,5]oxadiazolo[3,4-b]pyridin-carboxylat
DK4153599T3 (da) 2020-05-22 2024-06-17 Boehringer Ingelheim Int Fremgangsmåde til at fremstille alkyl 7-amino-5-methyl-[1,2,5]oxadiazolo[3,4-b]pyridin-carboxylat
US12091412B2 (en) * 2020-06-16 2024-09-17 Volastra Therapeutics, Inc. Heterocyclic inhibitors of ENPP1
CN115073363B (zh) * 2022-06-16 2024-01-26 宁波申泰生物科技有限公司 一种5-氟-2-甲氧基烟醛及其制备方法

Family Cites Families (37)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3338292A1 (de) * 1983-10-21 1985-05-02 Basf Ag, 6700 Ludwigshafen 7-amino-azolo(1,5-a)-pyrimidine und diese enthaltende fungizide
JP2002249492A (ja) 2000-12-22 2002-09-06 Nippon Bayer Agrochem Co Ltd トリアゾロピリミジン類
WO2004082383A1 (en) 2003-03-17 2004-09-30 Basf Aktiengesellschaft Use of triazolopyrimidines for combating nematode diseases of plants
WO2006114405A2 (de) 2005-04-25 2006-11-02 Basf Aktiengesellschaft Verwendung von 5-alkyl-6-phenylalkyl-7-amino-azolopyrimidinen, neue azolopyrimidine, verfahren zu ihrer herstellung und sie enthaltende mittel
AU2008216265B2 (en) 2007-02-15 2014-04-03 Indiana University Research And Technology Corporation Glucagon/GLP-1 receptor co-agonists
DK3567035T3 (da) 2007-04-11 2022-09-05 Canbas Co Ltd N-substituerede 2,5-dioxo-azolin-forbindelser til anvendelse ved behandling af cancer
CA2685524A1 (en) * 2007-04-30 2008-11-06 Abbott Laboratories Inhibitors of diacylglycerol o-acyltransferase type 1 enzyme
CA2687611A1 (en) 2007-05-24 2008-11-27 Bayer Schering Pharma Aktiengesellschaft Novel sulphoximine-substituted quinoline and quinazoline derivatives as kinase inhibitors
US7994122B2 (en) 2007-06-15 2011-08-09 Zealand Pharma A/S Glucagon analogues
FR2934058B1 (fr) 2008-07-15 2010-09-24 Centre Nat Rech Scient Dispositif de projection interferometrique a trois ouvertures pour produire une tache constituee de structures fines
FR2933989B1 (fr) 2008-07-16 2013-03-08 Commissariat Energie Atomique Procede de purification de microorganismes presents dans des echantillons liquides
FR2933975B1 (fr) 2008-07-17 2011-02-18 Servier Lab Nouveau procede de preparation de benzocyclobutenes fonctionnalises,et application a la synthese de l'ivabradine et de ses sels d'addition a un acide pharmaceutiquement acceptable.
AU2008365555B2 (en) 2008-12-15 2016-01-14 Zealand Pharma A/S Glucagon analogues
MX2011006320A (es) 2008-12-15 2011-09-22 Zealand Pharma As Analogos de glucagon.
EP2370462B1 (en) 2008-12-15 2014-07-16 Zealand Pharma A/S Glucagon analogues
KR20110126592A (ko) 2008-12-15 2011-11-23 질랜드 파마 에이/에스 글루카곤 유사체
AP3329A (en) 2009-07-13 2015-06-30 Zealand Pharma As Acylated glucagon analogues
US20110078154A1 (en) 2009-09-28 2011-03-31 Accenture Global Services Gmbh Recruitment screening tool
WO2011114148A1 (en) 2010-03-17 2011-09-22 Astrazeneca Ab 4h- [1, 2, 4] triazolo [5, 1 -b] pyrimidin-7 -one derivatives as ccr2b receptor antagonists
AR081975A1 (es) 2010-06-23 2012-10-31 Zealand Pharma As Analogos de glucagon
AU2011269430A1 (en) 2010-06-24 2013-01-10 Zealand Pharma A/S Glucagon analogues
HK1200369A1 (en) 2011-12-23 2015-10-09 Zealand Pharma A/S Glucagon analogues
CN104254525B (zh) * 2012-02-24 2016-05-25 武田药品工业株式会社 芳环化合物
US9492448B2 (en) 2012-06-20 2016-11-15 University Of Virginia Patent Foundation Compositions and methods for regulating glucose homeostasis and insulin action
TWI608013B (zh) 2012-09-17 2017-12-11 西蘭製藥公司 升糖素類似物
UA118034C2 (uk) 2013-11-14 2018-11-12 Елі Ліллі Енд Компані Заміщений піперидилетилпіримідин як інгібітор грелін-o-ацилтрансферази
EP3193939A4 (en) 2014-09-17 2018-10-24 The Regents of The University of California Small lipopeptidomimetic inhibitors of ghrelin o-acyl transferase
JP6615896B2 (ja) 2015-01-30 2019-12-04 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング アルドステロン合成酵素阻害剤
AR104672A1 (es) 2015-04-15 2017-08-09 Lilly Co Eli Inhibidores de grelina o-aciltransferasa
AR104673A1 (es) 2015-04-15 2017-08-09 Lilly Co Eli Inhibidores de grelina o-aciltransferasa
CA3002831C (en) 2015-10-22 2024-04-16 Cavion, Inc. Methods for treating angelman syndrome and related disorders
EA037277B1 (ru) 2016-08-05 2021-03-03 Бёрингер Ингельхайм Интернациональ Гмбх Производные оксадиазолопиридина для применения в качестве ингибиторов грелин-о-ацилтрасферазы (goat)
WO2018044663A1 (en) 2016-08-29 2018-03-08 Merck Sharp & Dohme Corp. Novel substituted n'-hydroxycarbamimidoyl-1,2,5-oxadiazole compounds as indoleamine 2,3-dioxygenase (ido) inhibitors
JOP20200187A1 (ar) * 2018-02-02 2020-07-29 Boehringer Ingelheim Int مشتقات ترايازولو بيريميدين للاستخدام كمثبطات جريلين o- أسيل ترانسفيراز (goat)
US11136337B2 (en) 2018-02-02 2021-10-05 Boehringer Ingelheim International Gmbh Pyrazole- and indazole-substituted oxadiazolopyridine derivatives for use as ghrelin O-acyl transferase (GOAT) inhibitors
MX2020008053A (es) 2018-02-02 2020-09-07 Boehringer Ingelheim Int Derivados de oxadiazolopiridina sustituidos con bencilo, (piridin-3-il)metilo o (piridin-4-il)metilo como inhibidores de ghrelin o-aciltransferasa (goat).
AU2019215709A1 (en) 2018-02-02 2020-07-16 Boehringer Ingelheim International Gmbh Heterocyclyl-substituted oxadiazolopyridine derivatives for use as ghrelin O-acyl transferase (GOAT) inhibitors

Also Published As

Publication number Publication date
EP3746443B1 (en) 2022-07-06
US11583532B2 (en) 2023-02-21
WO2019149660A1 (en) 2019-08-08
CN111683951B (zh) 2023-10-13
CL2020001909A1 (es) 2020-10-30
IL276145A (en) 2020-09-30
CR20200329A (es) 2020-09-04
ECSP20050797A (es) 2020-09-30
JP7083397B2 (ja) 2022-06-10
EP3746443A1 (en) 2020-12-09
CN111683951A (zh) 2020-09-18
EA202091803A1 (ru) 2020-12-16
KR20200118125A (ko) 2020-10-14
JOP20200187A1 (ar) 2020-07-29
SG11202006302TA (en) 2020-07-29
JP2021512115A (ja) 2021-05-13
BR112020014436A2 (pt) 2020-12-01
PH12020551170A1 (en) 2021-05-31
AU2019215710A1 (en) 2020-07-23
CA3087925A1 (en) 2019-08-08
US20210038603A1 (en) 2021-02-11
MX2020007994A (es) 2020-09-09
MA51774A (fr) 2021-05-12
CO2020009177A2 (es) 2020-07-31

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