PE20170664A1 - Agonistas del receptor de apelina(apj) y usos de los mismos - Google Patents
Agonistas del receptor de apelina(apj) y usos de los mismosInfo
- Publication number
- PE20170664A1 PE20170664A1 PE2016002511A PE2016002511A PE20170664A1 PE 20170664 A1 PE20170664 A1 PE 20170664A1 PE 2016002511 A PE2016002511 A PE 2016002511A PE 2016002511 A PE2016002511 A PE 2016002511A PE 20170664 A1 PE20170664 A1 PE 20170664A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- apj
- apeline
- same
- receptor agonists
- Prior art date
Links
Classifications
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- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
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- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
- A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
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- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/42—Oxazoles
- A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
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- 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
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- 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
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- 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
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- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
- C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
- C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D277/36—Sulfur atoms
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- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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- 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
- C07D403/06—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 linked by a carbon chain containing only aliphatic carbon atoms
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- 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
- C07D403/12—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 linked by a chain containing hetero atoms as chain links
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- C07—ORGANIC CHEMISTRY
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- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
- C07D407/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
- C07D407/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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- 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
- C07D413/12—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 linked by a chain containing hetero atoms as chain links
Abstract
Se refiere a un compuesto de formula I, donde: R1 es fenilo sustituido; R2 es alquilo C1-C8, heteroarilo, entre otros; R3 es alquilo C1-C8, alquil C1-C8-cicloalquil C3-C8 o cicloalquil C3-C8; R4, R5 y R6 son independientemente adamantanilo, arilo, alquilo C1-C8, entre otros; Z es H2 u =O. Son compuestos preferidos: acido (S)-2-ciclohexil-2-(5-(2,6-dimetoxifenil)-1-(4-fluorofenil)-1H-pirazol-3-carboxamido)acetico; acido (S)-3-(5-(2,6-dimetoxifenil)1-(4-fluorofenil)-1H-pirazol-3-carboxamido)-5-metilhexanoico; entre otros. Tambien se refiere a una composicion farmaceutica. Dichos compuestos son agonistas del receptor de apelina (APJ), siendo utiles en el tratamiento de asma, cardiomiopatia, diabetes, entre otros
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201462008688P | 2014-06-06 | 2014-06-06 | |
PCT/US2015/034427 WO2015188073A1 (en) | 2014-06-06 | 2015-06-05 | Apelin receptor (apj) agonists and uses thereof |
Publications (1)
Publication Number | Publication Date |
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PE20170664A1 true PE20170664A1 (es) | 2017-06-10 |
Family
ID=53524940
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PE2016002511A PE20170664A1 (es) | 2014-06-06 | 2015-06-05 | Agonistas del receptor de apelina(apj) y usos de los mismos |
Country Status (15)
Country | Link |
---|---|
US (2) | US10377718B2 (es) |
EP (1) | EP3152200A1 (es) |
JP (1) | JP6767878B2 (es) |
KR (1) | KR102509043B1 (es) |
CN (1) | CN106459004B (es) |
AU (1) | AU2015269247B2 (es) |
BR (1) | BR112016028119A2 (es) |
CA (1) | CA2949559C (es) |
IL (1) | IL248988A0 (es) |
MA (1) | MA39999A (es) |
MX (1) | MX2016014890A (es) |
PE (1) | PE20170664A1 (es) |
RU (1) | RU2705800C2 (es) |
WO (1) | WO2015188073A1 (es) |
ZA (1) | ZA201607850B (es) |
Families Citing this family (27)
Publication number | Priority date | Publication date | Assignee | Title |
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US20170174633A1 (en) * | 2014-03-25 | 2017-06-22 | Research Triangle Institute | Pyrazole compounds selective for neurotensin 2 receptor |
RU2705800C2 (ru) | 2014-06-06 | 2019-11-12 | Рисерч Трайэнгл Инститьют | Агонисты рецептора апелина (apj) и их применение |
GB201415569D0 (en) | 2014-09-03 | 2014-10-15 | C4X Discovery Ltd | Therapeutic Compounds |
WO2016176473A1 (en) * | 2015-04-28 | 2016-11-03 | Sanford-Burnham Medical Researc Institute | Apelin receptor agonists and methods of use thereof |
EP3300500B9 (en) | 2015-05-20 | 2021-01-13 | Amgen Inc. | Triazole agonists of the apj receptor |
KR20180067599A (ko) * | 2015-10-14 | 2018-06-20 | 브리스톨-마이어스 스큅 컴퍼니 | Apj 효능제로서의 2,4-디히드록시-니코틴아미드 |
WO2017100558A1 (en) | 2015-12-09 | 2017-06-15 | Research Triangle Institute | Improved apelin receptor (apj) agonists and uses thereof |
CA3008630A1 (en) * | 2015-12-16 | 2017-06-22 | Bristol-Myers Squibb Company | Heteroarylhydroxypyrimidinones as agonists of the apj receptor |
GB201601703D0 (en) | 2016-01-29 | 2016-03-16 | C4X Discovery Ltd | Therapeutic compounds |
WO2017165640A1 (en) * | 2016-03-24 | 2017-09-28 | Bristol-Myers Squibb Company | 6-hydroxy-4-oxo-1,4-dihydropyrimidine-5-carboxamides as apj agonists |
EP3452466B1 (en) | 2016-05-03 | 2020-08-12 | Amgen Inc. | Heterocyclic triazole compounds as agonists of the apj receptor |
CN114507217A (zh) * | 2016-10-12 | 2022-05-17 | 三角研究所 | 杂环爱帕琳肽受体(apj)激动剂及其用途 |
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 |
CN110072531A (zh) | 2016-10-19 | 2019-07-30 | 阿维夫公司 | 用于治疗心血管相关疾病的爱帕琳的新型聚乙二醇化的脂质体制剂 |
WO2018093580A1 (en) | 2016-11-16 | 2018-05-24 | Amgen Inc. | Triazole pyridyl compounds as agonists of the apj receptor |
WO2018093577A1 (en) | 2016-11-16 | 2018-05-24 | 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 |
US10906890B2 (en) | 2016-11-16 | 2021-02-02 | Amgen Inc. | Triazole phenyl compounds as agonists of the APJ receptor |
EP3541792B1 (en) | 2016-11-16 | 2020-12-23 | Amgen Inc. | Triazole furan compounds as agonists of the apj receptor |
WO2018097945A1 (en) | 2016-11-16 | 2018-05-31 | Amgen Inc. | Heteroaryl-substituted triazoles as apj receptor agonists |
WO2018207881A1 (ja) * | 2017-05-12 | 2018-11-15 | 武田薬品工業株式会社 | 複素環化合物 |
EP3704122B1 (en) | 2017-11-03 | 2021-09-01 | Amgen Inc. | Fused triazole agonists of the apj receptor |
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AU2015269247A1 (en) | 2016-12-01 |
WO2015188073A1 (en) | 2015-12-10 |
CA2949559A1 (en) | 2015-12-10 |
CN106459004A (zh) | 2017-02-22 |
US20190315693A1 (en) | 2019-10-17 |
ZA201607850B (en) | 2018-05-30 |
MX2016014890A (es) | 2017-05-01 |
RU2016144329A3 (es) | 2018-11-23 |
CN106459004B (zh) | 2020-09-15 |
IL248988A0 (en) | 2017-01-31 |
RU2016144329A (ru) | 2018-07-11 |
US11401244B2 (en) | 2022-08-02 |
US20160207889A1 (en) | 2016-07-21 |
BR112016028119A2 (pt) | 2017-08-22 |
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