PE20181487A1 - Heteroarilhidroxipirimidinonas como agonistas del receptor de apelina (apj) - Google Patents
Heteroarilhidroxipirimidinonas como agonistas del receptor de apelina (apj)Info
- Publication number
- PE20181487A1 PE20181487A1 PE2018001129A PE2018001129A PE20181487A1 PE 20181487 A1 PE20181487 A1 PE 20181487A1 PE 2018001129 A PE2018001129 A PE 2018001129A PE 2018001129 A PE2018001129 A PE 2018001129A PE 20181487 A1 PE20181487 A1 PE 20181487A1
- Authority
- PE
- Peru
- Prior art keywords
- apj
- heteroarylhydroxypirimidinones
- receptor agonists
- compounds
- apelin receptor
- Prior art date
Links
- 102100030949 Apelin receptor Human genes 0.000 title 2
- 108091008803 APLNR Proteins 0.000 title 1
- 239000000018 receptor agonist Substances 0.000 title 1
- 229940044601 receptor agonist Drugs 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 2
- -1 5- (benzo [d] isoxazol-3-ylmethyl) -1,3,4-oxadiazol-2-yl Chemical group 0.000 abstract 2
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 1
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 abstract 1
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 1
- 206010019280 Heart failures Diseases 0.000 abstract 1
- UQSPDQBZYCFYTL-UHFFFAOYSA-N O1N=C(C2=C1C=CC=C2)CC1=NN=C(O1)C=1C(N=C(N(C=1O)C1=C(C=CC=C1OC)OC)CCCC)=O Chemical compound O1N=C(C2=C1C=CC=C2)CC1=NN=C(O1)C=1C(N=C(N(C=1O)C1=C(C=CC=C1OC)OC)CCCC)=O UQSPDQBZYCFYTL-UHFFFAOYSA-N 0.000 abstract 1
- 208000006011 Stroke Diseases 0.000 abstract 1
- 239000000556 agonist Substances 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 125000004452 carbocyclyl group Chemical group 0.000 abstract 1
- 208000029078 coronary artery disease Diseases 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
Classifications
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- 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
- C07D403/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
- A61K31/495—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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic 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
- A61K31/495—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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- 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
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Cardiology (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Heart & Thoracic Surgery (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Hospice & Palliative Care (AREA)
- Epidemiology (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Agricultural Chemicals And Associated Chemicals (AREA)
- Pyridine Compounds (AREA)
Abstract
Se refiere a compuestos de formula (I), donde: alk es C1-6 alquilo sustituido con 1-5 R7; el anillo A es un heteroarilo de 5 a 6 miembros; el anillo B se selecciona de C3-6 cicloalquilo, arilo, carbociclilo, entre otros; R1 se selecciona de H, halogeno, NO2, entre otros; R2 se selecciona de C1-5 alquilo sustituido con 0-3 Re donde Re se selecciona independientemente de C1-6 alquilo, C2-6 alquenilo, entre otros. Dichos compuestos son utiles como agonistas de APJ siendo utiles en el tratamiento de cardiopatia coronaria, apoplejia, insuficiencia cardiaca, entre otros. Entre los compuestos preferidos tenemos los siguientes: 5-(5-(benzo[d]isoxazol-3-ilmetil)-1,3,4-oxadiazol-2-il)-2-butil-1-(2,6-dimetoxifenil)-6-hidroxipirimidin-4(1H)-ona; 5-(5-(benzo[d]isoxazol-3-ilmetil)-1,3,4-oxadiazol-2-il)-2-butil-1-(2,6-diciclopropilfenil)-6-hidroxipirimidin-4(1H)-ona; entre otros.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562267997P | 2015-12-16 | 2015-12-16 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20181487A1 true PE20181487A1 (es) | 2018-09-18 |
Family
ID=57708840
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2018001129A PE20181487A1 (es) | 2015-12-16 | 2016-12-15 | Heteroarilhidroxipirimidinonas como agonistas del receptor de apelina (apj) |
Country Status (21)
| Country | Link |
|---|---|
| US (1) | US10669261B2 (es) |
| EP (1) | EP3390400B1 (es) |
| JP (1) | JP6948322B2 (es) |
| KR (1) | KR102742744B1 (es) |
| CN (1) | CN108602813B (es) |
| AR (1) | AR107061A1 (es) |
| AU (1) | AU2016372048B2 (es) |
| BR (1) | BR112018012112A2 (es) |
| CA (1) | CA3008630A1 (es) |
| CL (1) | CL2018001621A1 (es) |
| CO (1) | CO2018007221A2 (es) |
| EA (1) | EA036736B1 (es) |
| ES (1) | ES2854733T3 (es) |
| HK (1) | HK1255163A1 (es) |
| IL (1) | IL259947B (es) |
| MX (1) | MX380669B (es) |
| PE (1) | PE20181487A1 (es) |
| SG (1) | SG11201804674UA (es) |
| TW (1) | TW201725203A (es) |
| UY (1) | UY37026A (es) |
| WO (1) | WO2017106396A1 (es) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PH12017502158B1 (en) | 2015-06-03 | 2022-04-27 | Bristol Meyers Squibb Co | 4-hydroxy-3-(heteroaryl)pyridine-2-one apj agonists for use in the treatment of cardiovascular disorders |
| TW201720796A (zh) | 2015-10-14 | 2017-06-16 | 必治妥美雅史谷比公司 | 作為apj促效劑之2,4-二羥基菸鹼醯胺 |
| HK1255162A1 (zh) | 2015-12-04 | 2019-08-09 | Bristol-Myers Squibb Company | 爱帕琳肽受体激动剂及使用方法 |
| SI3390395T1 (sl) | 2015-12-16 | 2020-11-30 | Loxo Oncology, Inc. | Spojine uporabne kot inhibitorji kinaz |
| EA037162B1 (ru) | 2016-03-24 | 2021-02-12 | Бристол-Маерс Сквибб Компани | 6-гидрокси-4-оксо-1,4-дигидропиримидин-5-карбоксамиды в качестве агонистов apj |
| WO2017192485A1 (en) | 2016-05-03 | 2017-11-09 | Amgen Inc. | Heterocyclic triazole compounds as agonists of the apj receptor |
| EP3468956B1 (en) * | 2016-06-14 | 2021-03-03 | Bristol-Myers Squibb Company | 6-hydroxy-5-(phenyl/heteroarylsulfonyl)pyrimidin-4(1h)-ones as apj agonists |
| US10889565B2 (en) | 2016-06-14 | 2021-01-12 | Bristol-Myers Squibb Company | 4-hydroxy-3-sulfonylpyridin-2(1H)-ones as APJ receptor agonists |
| CN110072850B (zh) | 2016-10-14 | 2023-07-21 | 百时美施贵宝公司 | 3-磺酰基-5-氨基吡啶-2,4-二醇apj激动剂 |
| US11046680B1 (en) | 2016-11-16 | 2021-06-29 | Amgen Inc. | Heteroaryl-substituted triazoles as APJ receptor agonists |
| US10736883B2 (en) | 2016-11-16 | 2020-08-11 | Amgen Inc. | Triazole furan compounds as agonists of the APJ receptor |
| US10906890B2 (en) | 2016-11-16 | 2021-02-02 | Amgen Inc. | Triazole phenyl compounds as agonists of the APJ receptor |
| EP3541803B1 (en) | 2016-11-16 | 2020-12-23 | Amgen Inc. | Triazole pyridyl compounds as agonists of the apj receptor |
| US11020395B2 (en) | 2016-11-16 | 2021-06-01 | Amgen Inc. | Cycloalkyl substituted triazole compounds as agonists of the APJ receptor |
| WO2018093576A1 (en) | 2016-11-16 | 2018-05-24 | Amgen Inc. | Alkyl substituted triazole compounds as agonists of the apj receptor |
| EP3788037A1 (en) | 2018-05-01 | 2021-03-10 | Amgen Inc. | Substituted pyrimidinones as agonists of the apj receptor |
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| US10570128B2 (en) * | 2014-05-28 | 2020-02-25 | Sanford Burnham Prebys Medical Discovery Institute | Agonists of the apelin receptor and methods of use thereof |
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| PH12017502158B1 (en) * | 2015-06-03 | 2022-04-27 | Bristol Meyers Squibb Co | 4-hydroxy-3-(heteroaryl)pyridine-2-one apj agonists for use in the treatment of cardiovascular disorders |
| TW201720796A (zh) | 2015-10-14 | 2017-06-16 | 必治妥美雅史谷比公司 | 作為apj促效劑之2,4-二羥基菸鹼醯胺 |
| HK1255162A1 (zh) | 2015-12-04 | 2019-08-09 | Bristol-Myers Squibb Company | 爱帕琳肽受体激动剂及使用方法 |
| EA037162B1 (ru) | 2016-03-24 | 2021-02-12 | Бристол-Маерс Сквибб Компани | 6-гидрокси-4-оксо-1,4-дигидропиримидин-5-карбоксамиды в качестве агонистов apj |
| EP3468956B1 (en) | 2016-06-14 | 2021-03-03 | Bristol-Myers Squibb Company | 6-hydroxy-5-(phenyl/heteroarylsulfonyl)pyrimidin-4(1h)-ones as apj agonists |
| US10889565B2 (en) | 2016-06-14 | 2021-01-12 | Bristol-Myers Squibb Company | 4-hydroxy-3-sulfonylpyridin-2(1H)-ones as APJ receptor agonists |
| CN110072850B (zh) | 2016-10-14 | 2023-07-21 | 百时美施贵宝公司 | 3-磺酰基-5-氨基吡啶-2,4-二醇apj激动剂 |
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2016
- 2016-12-15 BR BR112018012112-6A patent/BR112018012112A2/pt not_active Application Discontinuation
- 2016-12-15 MX MX2018007155A patent/MX380669B/es unknown
- 2016-12-15 ES ES16820507T patent/ES2854733T3/es active Active
- 2016-12-15 AU AU2016372048A patent/AU2016372048B2/en not_active Ceased
- 2016-12-15 JP JP2018531333A patent/JP6948322B2/ja active Active
- 2016-12-15 WO PCT/US2016/066750 patent/WO2017106396A1/en not_active Ceased
- 2016-12-15 KR KR1020187019799A patent/KR102742744B1/ko active Active
- 2016-12-15 HK HK18114280.0A patent/HK1255163A1/zh unknown
- 2016-12-15 TW TW105141572A patent/TW201725203A/zh unknown
- 2016-12-15 CN CN201680081704.3A patent/CN108602813B/zh active Active
- 2016-12-15 US US16/061,365 patent/US10669261B2/en active Active
- 2016-12-15 CA CA3008630A patent/CA3008630A1/en not_active Abandoned
- 2016-12-15 SG SG11201804674UA patent/SG11201804674UA/en unknown
- 2016-12-15 UY UY0001037026A patent/UY37026A/es unknown
- 2016-12-15 EP EP16820507.8A patent/EP3390400B1/en active Active
- 2016-12-15 PE PE2018001129A patent/PE20181487A1/es unknown
- 2016-12-15 EA EA201891336A patent/EA036736B1/ru not_active IP Right Cessation
- 2016-12-15 AR ARP160103867A patent/AR107061A1/es unknown
-
2018
- 2018-06-11 IL IL259947A patent/IL259947B/en active IP Right Grant
- 2018-06-15 CL CL2018001621A patent/CL2018001621A1/es unknown
- 2018-07-11 CO CONC2018/0007221A patent/CO2018007221A2/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CL2018001621A1 (es) | 2018-08-03 |
| CN108602813B (zh) | 2021-10-29 |
| AR107061A1 (es) | 2018-03-14 |
| WO2017106396A1 (en) | 2017-06-22 |
| MX2018007155A (es) | 2018-08-15 |
| KR20180095577A (ko) | 2018-08-27 |
| US20180362508A1 (en) | 2018-12-20 |
| CN108602813A (zh) | 2018-09-28 |
| EP3390400A1 (en) | 2018-10-24 |
| KR102742744B1 (ko) | 2024-12-12 |
| JP6948322B2 (ja) | 2021-10-13 |
| MX380669B (es) | 2025-03-12 |
| EA201891336A1 (ru) | 2019-01-31 |
| HK1255163A1 (zh) | 2019-08-09 |
| CO2018007221A2 (es) | 2018-07-19 |
| BR112018012112A2 (pt) | 2018-12-04 |
| IL259947A (en) | 2018-07-31 |
| IL259947B (en) | 2020-10-29 |
| AU2016372048B2 (en) | 2021-02-04 |
| EA036736B1 (ru) | 2020-12-14 |
| EP3390400B1 (en) | 2021-01-20 |
| US10669261B2 (en) | 2020-06-02 |
| UY37026A (es) | 2017-06-30 |
| AU2016372048A1 (en) | 2018-08-02 |
| ES2854733T3 (es) | 2021-09-22 |
| SG11201804674UA (en) | 2018-06-28 |
| CA3008630A1 (en) | 2017-06-22 |
| JP2018538304A (ja) | 2018-12-27 |
| TW201725203A (zh) | 2017-07-16 |
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