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

Links

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

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 (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2874587T3 (es) 2016-08-05 2021-11-05 Boehringer Ingelheim Int Derivados de oxadiazolopiridina para su uso como inhibidores de la grelina O-aciltransferasa (GOAT)
CA3087925A1 (en) * 2018-02-02 2019-08-08 Boehringer Ingelheim International Gmbh Triazolopyrimidine derivatives for use as ghrelin o-acyl transferase (goat) inhibitors
EP3746451B1 (en) 2018-02-02 2023-07-12 Boehringer Ingelheim International GmbH Benzyl-, (pyridin-3-yl)methyl- or (pyridin-4-yl)methyl-substituted oxadiazolopyridine derivatives as ghrelin o-acyl transferase (goat) inhibitors
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
AU2021268606A1 (en) 2020-05-04 2022-12-15 Volastra Therapeutics, Inc. Imino sulfanone inhibitors of ENPP1
EP4153600A1 (en) 2020-05-22 2023-03-29 Boehringer Ingelheim International GmbH Continuous process for manufacturing alkyl 7-amino-5-methyl-[1,2,5]oxadiazolo[3,4-b]pyridine-carboxylate
JP2023526351A (ja) 2020-05-22 2023-06-21 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 アルキル7-アミノ-5-メチル-[1,2,5]オキサジアゾロ[3,4-b]ピリジンカルボキシレートの製造方法
WO2021257614A1 (en) * 2020-06-16 2021-12-23 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
CN101163404A (zh) * 2005-04-25 2008-04-16 巴斯福股份公司 5-烷基-6-苯基烷基-7-氨基唑并嘧啶的用途、新的唑并嘧啶、其制备方法以及包含它们的组合物
EA017849B1 (ru) 2007-02-15 2013-03-29 Индиана Юниверсити Рисерч Энд Текнолоджи Корпорейшн Соагонисты глюкагоновых/glp-1-рецепторов
IL309201A (en) 2007-04-11 2024-02-01 Canbas Co Ltd Compounds with anticancer activity
CA2685524A1 (en) 2007-04-30 2008-11-06 Abbott Laboratories Inhibitors of diacylglycerol o-acyltransferase type 1 enzyme
JP2010527951A (ja) 2007-05-24 2010-08-19 バイエル・シエーリング・ファーマ アクチエンゲゼルシャフト キナーゼ阻害剤としての新規なスルホキシイミン置換型キノリン及びキナゾリン誘導体
JP5385266B2 (ja) 2007-06-15 2014-01-08 ジーランド ファーマ アクティーゼルスカブ グルカゴン類似体
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.
US8642540B2 (en) 2008-12-15 2014-02-04 Zealand Pharma A/S Glucagon analogues
PL2370462T3 (pl) 2008-12-15 2015-01-30 Zealand Pharma As Analogi glukagonu
CA2747109A1 (en) 2008-12-15 2010-06-24 Zealand Pharma A/S Glucagon analogues
EA020497B1 (ru) 2008-12-15 2014-11-28 Зилэнд Фарма А/С Аналоги глюкагона
EA022816B1 (ru) 2009-07-13 2016-03-31 Зилэнд Фарма А/С Ацилированные аналоги глюкагона
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
UY33462A (es) 2010-06-23 2012-01-31 Zealand Pharma As Analogos de glucagon
CA2802897A1 (en) 2010-06-24 2011-12-29 Zealand Pharma A/S Glucagon analogues
EP2793931A2 (en) 2011-12-23 2014-10-29 Zealand Pharma A/S Glucagon analogues
ES2640258T3 (es) * 2012-02-24 2017-11-02 Takeda Pharmaceutical Company Limited Compuesto anular aromático como inhibidor de grelina o-aciltransferasa
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
US20170275249A1 (en) 2014-09-17 2017-09-28 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
AR104673A1 (es) 2015-04-15 2017-08-09 Lilly Co Eli Inhibidores de grelina o-aciltransferasa
AR104672A1 (es) 2015-04-15 2017-08-09 Lilly Co Eli Inhibidores de grelina o-aciltransferasa
MX2018004947A (es) 2015-10-22 2018-11-09 Cavion Inc Metodos para el tratamiento de sindrome de angelman y de los trastornos relacionados.
ES2874587T3 (es) 2016-08-05 2021-11-05 Boehringer Ingelheim Int Derivados de oxadiazolopiridina para su uso como inhibidores de la grelina O-aciltransferasa (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
EP3746451B1 (en) 2018-02-02 2023-07-12 Boehringer Ingelheim International GmbH Benzyl-, (pyridin-3-yl)methyl- or (pyridin-4-yl)methyl-substituted oxadiazolopyridine derivatives as ghrelin o-acyl transferase (goat) inhibitors
CA3087925A1 (en) 2018-02-02 2019-08-08 Boehringer Ingelheim International Gmbh Triazolopyrimidine derivatives for use as ghrelin o-acyl transferase (goat) inhibitors
WO2019149658A1 (en) 2018-02-02 2019-08-08 Boehringer Ingelheim International Gmbh Pyrazole- and indazole-substituted oxadiazolopyridine derivatives for use as ghrelin o-acyl transferase (goat) inhibitors
MX2020008116A (es) 2018-02-02 2020-09-25 Boehringer Ingelheim Int Derivados de oxadiazolopiridina sustituidos con heterociclilo para usar como inhibidores de ghrelin o-aciltransferasa (goat).

Also Published As

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

Similar Documents

Publication Publication Date Title
PE20210658A1 (es) Derivados de triazolopirimidina para usar como inhibidores de ghrelin o-aciltransferasa (goat)
PE20191613A1 (es) Compuestos de pirazolo[1,5-a]piridina sustituidos como inhibidores de la quinasa ret
PE20170663A1 (es) Compuestos de 5- cloro- 2- difluorometoxifenil pirazolopirimidina, composiciones y metodos de uso de los mismos
PE20120534A1 (es) PIRIMIDINAS FUSIONADAS COMO INHIBIDORES DE Akt
PE20171307A1 (es) Compuestos de triazolopirimidina y usos de los mismos
PE20170189A1 (es) Nuevos derivados de pirazolo pirimidina y su uso como inhibidores de malt1
AR112833A2 (es) Compuestos pirazolo[1,5-a]pirimidina sustituida como inhibidores de trk cinasa
PE20190918A1 (es) Compuestos de pirazolo[1,5-a]piridina sustituidos como inhibidores de la quinasa ret
PE20191540A1 (es) DERIVADOS DE PIRROLO [1,2-b] PIRIDAZINA
PE20151249A1 (es) Derivados de pirazolopirimidina como inhibidores de jak quinasas
PE20090370A1 (es) Derivados de heterociclo fusionado como inhibidores de quinasa
MX2020008559A (es) Compuestos heterocíclicos como inhibidores de la quinasa.
CU20210015A7 (es) COMPUESTOS DE PIRAZOLO [3.4-b] PIRIDINA COMO INHIBIDORES DE CINASAS TAM Y MET
PE20110828A1 (es) Compuestos de pirazolopirimidina como inhibidores de jak
PE20120121A1 (es) Derivados de imidazopirazina como inhibidores de syk
PE20170666A1 (es) 2-(morfolin-4-il)-1,7-naftiridinas
PE20141059A1 (es) Indazoles
SV2018005655A (es) "derivados de 8-[6-[3-(amino)propoxi]-3-piridil]1-isopropilimidazo[4,5-c]quinolin-2-ona como moduladores selectivos de la cinasa de la ataxia telangiectasia mutada (atm) para el tratamiento del cancer"
PE20161388A1 (es) Inhibidores de la jak1 para el tratamiento de sindromes mielodisplasicos
PE20140390A1 (es) Derivados de imidazo[1,2-b]piridazina e imidazo[4,5-b]piridina como inhibidores de jak
PE20121815A1 (es) Compuestos de pirrolo-pirimidina como inhibidores de cdk4/6
CL2010001486A1 (es) Compuestos derivados de [1,2,4]triazolo[1,5-a]piridina, inhibidores de jak; composicion farmaceutica; kit farmaceutico; su uso en el tratamiento de enfermedades tales como cancer, diabetes, enfermedad de alzheimer, enfermedad hepatica, trastornos del snc, entre otras.
PE20191236A1 (es) Compuestos de pirazolopirimidina y metodos de uso de los mismos
PE20110560A1 (es) NUEVOS DERIVADOS DE TRIAZOLO[4,3-a]PIRIDINA, SU PROCEDIMIENTO DE PREPARACION, SU APLICACION COMO MEDICAMENTOS, COMPOSICIONES FARMACEUTICAS Y NUEVA UTILIZACION PARTICULARMENTE COMO INHIBIDORES DE MET
NI200500174A (es) Beta-carboniles útiles para el tratamiento de enfermedades inflamatorias