EA202091804A1 - Гетероциклил-замещенные оксадиазолопиридиновые производные для применения в качестве ингибиторов грелин-о-ацилтрансферазы (goat) - Google Patents
Гетероциклил-замещенные оксадиазолопиридиновые производные для применения в качестве ингибиторов грелин-о-ацилтрансферазы (goat)Info
- Publication number
- EA202091804A1 EA202091804A1 EA202091804A EA202091804A EA202091804A1 EA 202091804 A1 EA202091804 A1 EA 202091804A1 EA 202091804 A EA202091804 A EA 202091804A EA 202091804 A EA202091804 A EA 202091804A EA 202091804 A1 EA202091804 A1 EA 202091804A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- acyltransferase
- goat
- grelin
- heterocyclyl
- inhibitors
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title 1
- RWXCVESEMJNNMF-UHFFFAOYSA-N oxadiazolo[5,4-b]pyridine Chemical class C1=CN=C2ON=NC2=C1 RWXCVESEMJNNMF-UHFFFAOYSA-N 0.000 title 1
- 102100038752 Ghrelin O-acyltransferase Human genes 0.000 abstract 2
- 101710205760 Ghrelin O-acyltransferase Proteins 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 208000008589 Obesity Diseases 0.000 abstract 1
- 230000006806 disease prevention Effects 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 208000030159 metabolic disease Diseases 0.000 abstract 1
- 235000020824 obesity Nutrition 0.000 abstract 1
- 230000000144 pharmacologic effect Effects 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
-
- 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
-
- 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
- A61K31/435—Heterocyclic 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
- A61K31/4353—Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- 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
- A61K31/435—Heterocyclic 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
-
- 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
- A61K31/495—Heterocyclic 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
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Diabetes (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Hematology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Obesity (AREA)
- General Chemical & Material Sciences (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Child & Adolescent Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Настоящее изобретение относится к соединениям общей формулы Iгде переменные X, R1, n, p и q имеют определения, приведенные в пункте 1, которые обладают ценными фармакологическими свойствами, в частности связываются с грелин-O-ацилтрансферазой (GOAT) и модулируют ее активность. Соединения пригодны для лечения и предотвращения заболеваний, на которые может влиять этот рецептор, таких как метаболические заболевания, в частности ожирение.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP18154828 | 2018-02-02 | ||
| PCT/EP2019/051993 WO2019149659A1 (en) | 2018-02-02 | 2019-01-28 | Heterocyclyl-substituted oxadiazolopyridine derivatives for use as ghrelin o-acyl transferase (goat) inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| EA202091804A1 true EA202091804A1 (ru) | 2020-12-24 |
Family
ID=61157053
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA202091804A EA202091804A1 (ru) | 2018-02-02 | 2019-01-28 | Гетероциклил-замещенные оксадиазолопиридиновые производные для применения в качестве ингибиторов грелин-о-ацилтрансферазы (goat) |
Country Status (21)
| Country | Link |
|---|---|
| US (1) | US11319310B2 (ru) |
| EP (1) | EP3746450B1 (ru) |
| JP (1) | JP7150032B2 (ru) |
| KR (1) | KR20200118124A (ru) |
| CN (1) | CN111655699B (ru) |
| AU (1) | AU2019215709A1 (ru) |
| BR (1) | BR112020014320A2 (ru) |
| CA (1) | CA3087827A1 (ru) |
| CL (1) | CL2020001908A1 (ru) |
| CO (1) | CO2020009179A2 (ru) |
| CR (1) | CR20200331A (ru) |
| EA (1) | EA202091804A1 (ru) |
| EC (1) | ECSP20050791A (ru) |
| IL (1) | IL276137A (ru) |
| JO (1) | JOP20200191A1 (ru) |
| MA (1) | MA53074A (ru) |
| MX (1) | MX2020008116A (ru) |
| PE (1) | PE20210175A1 (ru) |
| PH (1) | PH12020551169A1 (ru) |
| SG (1) | SG11202006300XA (ru) |
| WO (1) | WO2019149659A1 (ru) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SG11201811804QA (en) * | 2016-08-05 | 2019-01-30 | Boehringer Ingelheim Int | Oxadiazolopyridine derivates for use as ghrelin o-acyl transferase (goat) inhibitors |
| CN111630055B (zh) * | 2018-02-02 | 2023-07-14 | 勃林格殷格翰国际有限公司 | 用作饥饿素o-酰基转移酶(goat)抑制剂的吡唑取代的和吲唑取代的噁二唑并吡啶衍生物 |
| EP3746443B1 (en) | 2018-02-02 | 2022-07-06 | Boehringer Ingelheim International GmbH | Triazolopyrimidine derivatives for use as ghrelin o-acyl transferase (goat) inhibitors |
| BR112020013082A2 (pt) | 2018-02-02 | 2020-12-01 | Boehringer Ingelheim International Gmbh | derivados de oxadiazolopiridina benzil-, (piridin-3-il)metil- ou (piridin-4-il)metil- substituídos como inibidores de grelina o-acil transferase (goat) |
| EP4153599B1 (en) | 2020-05-22 | 2024-03-13 | Boehringer Ingelheim International GmbH | Process for manufacturing alkyl 7-amino-5-methyl-[1,2,5]oxadiazolo[3,4-b]pyridine-carboxylate |
| WO2021233884A1 (en) | 2020-05-22 | 2021-11-25 | Boehringer Ingelheim International Gmbh | Continuous process for manufacturing alkyl 7-amino-5-methyl-[1,2,5]oxadiazolo[3,4-b]pyridine-carboxylate |
Family Cites Families (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2004082383A1 (en) | 2003-03-17 | 2004-09-30 | Basf Aktiengesellschaft | Use of triazolopyrimidines for combating nematode diseases of plants |
| MX2009008241A (es) | 2007-02-15 | 2009-10-08 | Univ Indiana Res & Tech Corp | Co-agonistas de receptor de glucagon/glp-1. |
| EP2158214B1 (en) | 2007-06-15 | 2011-08-17 | Zealand Pharma A/S | Glucagon analogues |
| JP5635531B2 (ja) | 2008-12-15 | 2014-12-03 | 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 |
| MY160219A (en) | 2008-12-15 | 2017-02-28 | Zealand Pharma As | Glucagon analogues |
| WO2010070252A1 (en) | 2008-12-15 | 2010-06-24 | Zealand Pharma A/S | Glucagon analogues |
| WO2010070255A1 (en) | 2008-12-15 | 2010-06-24 | Zealand Pharma A/S | Glucagon analogues |
| EA022816B1 (ru) | 2009-07-13 | 2016-03-31 | Зилэнд Фарма А/С | Ацилированные аналоги глюкагона |
| AR081975A1 (es) | 2010-06-23 | 2012-10-31 | Zealand Pharma As | Analogos de glucagon |
| EP2585482B1 (en) | 2010-06-24 | 2019-03-27 | Zealand Pharma A/S | Glucagon analogues |
| US20130316941A1 (en) | 2011-12-23 | 2013-11-28 | Boehringer Ingelheim International Gmbh | Glucagon analogues |
| EP2838891B1 (en) | 2012-02-24 | 2017-08-02 | Takeda Pharmaceutical Company Limited | Aromatic ring compound as ghrelin o-acyltransferase inhibitor |
| ES2784223T3 (es) * | 2012-06-20 | 2020-09-23 | Univ Virginia Patent Foundation | Composiciones y procedimientos para regular la homeostasis de glucosa y la acción de insulina |
| 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 |
| WO2016044467A1 (en) | 2014-09-17 | 2016-03-24 | The Regents Of The University Of California | Small lipopeptidomimetic inhibitors of ghrelin o-acyl transferase |
| EP3250569B1 (en) | 2015-01-30 | 2019-01-09 | Boehringer Ingelheim International GmbH | Aldosterone synthase inhibitors |
| 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 |
| SG11201811804QA (en) * | 2016-08-05 | 2019-01-30 | Boehringer Ingelheim Int | Oxadiazolopyridine derivates for use as ghrelin o-acyl transferase (goat) inhibitors |
-
2019
- 2019-01-28 MX MX2020008116A patent/MX2020008116A/es unknown
- 2019-01-28 PE PE2020001163A patent/PE20210175A1/es unknown
- 2019-01-28 CN CN201980010384.6A patent/CN111655699B/zh active Active
- 2019-01-28 US US16/966,489 patent/US11319310B2/en active Active
- 2019-01-28 WO PCT/EP2019/051993 patent/WO2019149659A1/en unknown
- 2019-01-28 KR KR1020207025418A patent/KR20200118124A/ko unknown
- 2019-01-28 SG SG11202006300XA patent/SG11202006300XA/en unknown
- 2019-01-28 EP EP19702085.2A patent/EP3746450B1/en active Active
- 2019-01-28 CA CA3087827A patent/CA3087827A1/en not_active Abandoned
- 2019-01-28 JP JP2020541870A patent/JP7150032B2/ja active Active
- 2019-01-28 BR BR112020014320-0A patent/BR112020014320A2/pt not_active Application Discontinuation
- 2019-01-28 AU AU2019215709A patent/AU2019215709A1/en not_active Abandoned
- 2019-01-28 CR CR20200331A patent/CR20200331A/es unknown
- 2019-01-28 MA MA053074A patent/MA53074A/fr unknown
- 2019-01-28 JO JOP/2020/0191A patent/JOP20200191A1/ar unknown
- 2019-01-28 EA EA202091804A patent/EA202091804A1/ru unknown
-
2020
- 2020-07-19 IL IL276137A patent/IL276137A/en unknown
- 2020-07-21 CL CL2020001908A patent/CL2020001908A1/es unknown
- 2020-07-24 CO CONC2020/0009179A patent/CO2020009179A2/es unknown
- 2020-07-31 PH PH12020551169A patent/PH12020551169A1/en unknown
- 2020-08-24 EC ECSENADI202050791A patent/ECSP20050791A/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| US20210040077A1 (en) | 2021-02-11 |
| BR112020014320A2 (pt) | 2020-12-08 |
| WO2019149659A1 (en) | 2019-08-08 |
| EP3746450B1 (en) | 2022-03-16 |
| CN111655699A (zh) | 2020-09-11 |
| CO2020009179A2 (es) | 2020-07-31 |
| JP7150032B2 (ja) | 2022-10-07 |
| SG11202006300XA (en) | 2020-07-29 |
| MA53074A (fr) | 2021-05-12 |
| EP3746450A1 (en) | 2020-12-09 |
| JOP20200191A1 (ar) | 2020-07-29 |
| MX2020008116A (es) | 2020-09-25 |
| IL276137A (en) | 2020-09-30 |
| ECSP20050791A (es) | 2020-09-30 |
| CL2020001908A1 (es) | 2020-10-30 |
| CR20200331A (es) | 2020-09-03 |
| AU2019215709A1 (en) | 2020-07-16 |
| JP2021512112A (ja) | 2021-05-13 |
| KR20200118124A (ko) | 2020-10-14 |
| PH12020551169A1 (en) | 2021-05-31 |
| CA3087827A1 (en) | 2019-08-08 |
| CN111655699B (zh) | 2023-07-14 |
| US11319310B2 (en) | 2022-05-03 |
| PE20210175A1 (es) | 2021-01-29 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| EA202091804A1 (ru) | Гетероциклил-замещенные оксадиазолопиридиновые производные для применения в качестве ингибиторов грелин-о-ацилтрансферазы (goat) | |
| EA202091803A1 (ru) | Производные триазолопиримидина для применения в качестве ингибиторов грелин-о-ацилтрансферазы (goat) | |
| EA201990418A1 (ru) | Производные оксадиазолопиридина для применения в качестве ингибиторов грелин-о-ацилтрасферазы (goat) | |
| EA202092896A1 (ru) | Гетероциклические и гетероарильные соединения для лечения болезни гентингтона | |
| EA201992253A1 (ru) | Новые гетероциклические производные, применимые в качестве ингибиторов shp2 | |
| PH12018500177A1 (en) | Compositions useful for treating disorders related to kit and pdfgr | |
| EA201891974A1 (ru) | Ингибиторы связывания белка wdr5 с белками | |
| EA201891910A1 (ru) | Гетероарильные ингибиторы pad4 | |
| EA201792205A1 (ru) | Гетероциклические соединения как ингибиторы lsd1 | |
| EA202090256A1 (ru) | 5-членные и бициклические гетероциклические амиды в качестве ингибиторов rock | |
| EA201890338A1 (ru) | Оксадиазольные производные, пригодные в качестве ингибиторов hdac | |
| EA202091805A1 (ru) | Бензил-, (пиридин-3-ил)метил- или (пиридин-4-ил)метил-замещенные оксадиазолопиридиновые производные в качестве ингибиторов грелин-о-ацилтрансферазы (goat) | |
| EA201592033A1 (ru) | 3-(2-АМИНОПИРИМИДИН-4-ИЛ)-5-(3-ГИДРОКСИПРОПИНИЛ)-1H-ПИРРОЛО[2,3-c]ПИРИДИНОВЫЕ ПРОИЗВОДНЫЕ В КАЧЕСТВЕ ИНГИБИТОРОВ NIK ДЛЯ ЛЕЧЕНИЯ РАКА | |
| EA201790817A1 (ru) | 2-амино-3,5-дифтор-3,6-диметил-6-фенил-3,4,5,6-тетрагидропиридины как ингибиторы bace1 для лечения болезни альцгеймера | |
| EA201790818A1 (ru) | 2-амино-6-(дифторметил)-5,5-дифтор-6-фенил-3,4,5,6-тетрагидропиридины как ингибиторы bace1 | |
| EA202190464A1 (ru) | Замещенные бензимидазолы в качестве ингибиторов pad4 | |
| EA202091428A1 (ru) | Замещенные амиды ii пирролидина | |
| EA202190272A1 (ru) | Дополнительно замещенные производные триазолохиноксалина | |
| EA202090414A1 (ru) | Соединения и их применение | |
| EA201600113A1 (ru) | Новые производные азабензимидазола | |
| EA201692260A1 (ru) | Соединения 1,3,4-тиадиазола и их применение в лечении рака | |
| EA202190271A1 (ru) | Замещенные триазолохиноксалиновые производные | |
| EA201692216A1 (ru) | Пирролидиновые модуляторы gpr40 для лечения заболеваний, таких как диабет | |
| EA202091429A1 (ru) | Замещенные амиды i пирролидина | |
| MX2023001906A (es) | Diarilureas como moduladores alostericos de cannabinoide cb1. |