AR104884A1 - Compuestos de 4-hidroxi-3-(heteroaril)piridin-2-ona como agonistas de apj - Google Patents
Compuestos de 4-hidroxi-3-(heteroaril)piridin-2-ona como agonistas de apjInfo
- Publication number
- AR104884A1 AR104884A1 ARP160101639A ARP160101639A AR104884A1 AR 104884 A1 AR104884 A1 AR 104884A1 AR P160101639 A ARP160101639 A AR P160101639A AR P160101639 A ARP160101639 A AR P160101639A AR 104884 A1 AR104884 A1 AR 104884A1
- Authority
- AR
- Argentina
- Prior art keywords
- substituted
- alkyl
- independently selected
- cr4r4
- case
- Prior art date
Links
- 239000000556 agonist Substances 0.000 title abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 6
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 5
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 4
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 4
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 4
- 229910052736 halogen Inorganic materials 0.000 abstract 4
- 125000000623 heterocyclic group Chemical group 0.000 abstract 4
- 150000002367 halogens Chemical class 0.000 abstract 3
- 229910052757 nitrogen Inorganic materials 0.000 abstract 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 2
- 229910052794 bromium Inorganic materials 0.000 abstract 2
- 229910052801 chlorine Inorganic materials 0.000 abstract 2
- 229910052731 fluorine Inorganic materials 0.000 abstract 2
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 2
- 125000000547 substituted alkyl group Chemical group 0.000 abstract 2
- 125000006706 (C3-C6) carbocyclyl group Chemical group 0.000 abstract 1
- 208000024172 Cardiovascular disease Diseases 0.000 abstract 1
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical group C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 125000004452 carbocyclyl group Chemical group 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 150000001721 carbon Chemical group 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 229940079593 drug Drugs 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
Classifications
-
- 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
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- 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
- C07D401/04—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 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
- C07D413/02—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
- 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
-
- 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
- C07D417/02—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 two hetero rings
- C07D417/04—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 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
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Epidemiology (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Hospice & Palliative Care (AREA)
- Biomedical Technology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
Compuestos agonistas de APJ, que se pueden usar como medicamentos útiles en el tratamiento de enfermedades cardiovasculares. Reivindicación 1: Un compuesto caracterizado por la fórmula [1], o un estereoisómero, un tautómero o una sal de aquel aceptable desde el punto de vista farmacéutico, en donde: alk es C₁₋₆ alquilo sustituido con 0 - 5 Rᵉ; el anillo A se selecciona independientemente de los compuestos del grupo de fórmula [2]; el anillo B se selecciona independientemente de: los compuestos de fórmula [3], fórmula [4] y heteroarilo de 6 miembros; R¹ se selecciona independientemente de: halógeno, NO₂, -(CH₂)ₙORᵇ, (CH₂)ₙS(O)ₚRᶜ, -(CH₂)ₙC(=O)Rᵇ, -(CH₂)ₙNRᵃRᵃ, -(CH₂)ₙCN, -(CH₂)ₙC(=O)NRᵃRᵃ, -(CH₂)ₙNRᵃC(=O)Rᵇ, -(CH₂)ₙNRᵃC(=O)NRᵃRᵃ, -(CH₂)ₙNRᵃC(=O)ORᵇ, -(CH₂)ₙOC(=O)NRᵃRᵃ, -(CH₂)ₙC(=O)ORᵇ, -(CH₂)ₙS(O)ₚNRᵃRᵃ, (CH₂)ₙNRᵃS(O)ₚNRᵃRᵃ, -(CH₂)ₙNRᵃS(O)ₚRᶜ, C₁₋₄ alquilo sustituido con 0 - 3 Rᵉ, -(CH₂)ₙ-C₃₋₆ carbociclilo sustituido con 0 - 3 Rᵉ y -(CH₂)ₙ-heterociclilo sustituido con 0 - 3 Rᵉ; R² se selecciona independientemente de: C₁₋₅ alquilo sustituido con 0 - 3 Rᵉ; C₁₋₅ alquenilo sustituido con 0 - 3 Rᵉ, y C₁₋₆ cicloalquilo sustituido con 0 - 3 Rᵉ; siempre que cuando R² es C₁₋₅ alquilo, los átomos de carbono, salvo el que está unido directamente al anillo de piridina, se puedan reemplazar por O, N y S; R³ se selecciona independientemente de: (1) -(CR⁴R⁴)ʳC(=O)OC₁₋₄, alquilo sustituido son 0 - 5 Rᵉ, (2) -(CR⁴R⁴)ʳNRᵃRᵃ, (3) -(CR⁴R⁴)ʳC(=O)NRᵃRᵃ, (4) -(CR⁴R⁴)ʳNRᵃC(=O)C₁₋₄ alquilo sustituido son 0 - 5 Rᵉ, (5) -(CR⁴R⁴)ʳNRᵃC(=O)(CR⁴R⁴)ₙOC₁₋₄ alquilo sustituido con 0 - 5 Rᵉ, (6) -(CR⁴R⁴)ʳ-R⁵, (7) -(CR⁴R⁴)ʳ-OR⁵, (8) -(CR⁴R⁴)ʳNRᵃC(=O)(CR⁴R⁴)ₙR⁵ y (9) -(CR⁴R⁴)ʳC(=O)NRᵃ(CR⁴R⁴)ₙR⁵; R⁴ se selecciona, independientemente de cada caso, de: H, halógeno, NRᵃRᵃ, OC₁₋₄ alquilo y C₁₋₄ alquilo; o R⁴ y R⁴, junto con el átomo de carbono al que están unidos, forman C₃₋₆ cicloalquilo sustituido con 0 - 5 Rᵉ; R⁵ se selecciona, independientemente de cada caso, de: -(CH₂)ₙC₃₋₁₀ carbociclo y -(CH₂)ₙ-heterociclo, cada uno sustituido con 0 - 3 R⁶; R⁶ se selecciona independientemente de: H, halógeno, =O, -(CH₂)ₙORᵇ, (CH₂)ₙS(O)ₚRᶜ, -(CH₂)ₙC(=O)Rᵇ, -(CH₂)ₙNRᵃRᵃ, -(CH₂)ₙCN, -(CH₂)ₙC(=O)NRᵃRᵃ, -(CH₂)ₙNRᵃC(=O)Rᵇ, -(CH₂)ₙNRᵃC(=O)NRᵃRᵃ, -(CH₂)ₙNRᵃC(=O)ORᵇ, -(CH₂)ₙOC(=O)NRᵃRᵃ, -(CH₂)ₙC(=O)ORᵇ, -(CH₂)ₙS(O)ₚNRᵃRᵃ, -(CH₂)ₙNRᵃS(O)ₚNRᵃRᵃ, -(CH₂)ₙNRᵃS(O)ₚRᶜ, C₁₋₅ alquilo sustituido con 0 - 3 Rᵉ, (CH₂)ₙ-C₃₋₆ carbociclilo sustituido con 0 - 3 Rᵉ y -(CH₂)ₙ-heterociclilo sustituido con 0 - 3 Rᵉ; Rᵃ, en cada caso, se selecciona independientemente de H, C₁₋₆ alquilo sustituido con 0 - 5 Rᵉ, C₂₋₆ alquenilo sustituido con 0 - 5 Rᵉ, C₂₋₆ alquinilo sustituido con 0 - 5 Rᵉ, -(CH₂)ₙ-C₃₋₁₀carbociclilo sustituido con 0 - 5 Rᵉ y -(CH₂)ₙ-heterociclilo sustituido con 0 - 5 Rᵉ; o Rᵃ y Rᵃ, junto con el átomo de nitrógeno al que están unidos, forman un anillo heterocíclico sustituido con 0 - 5 Rᵉ; Rᵇ, en cada caso, se selecciona independientemente de H, C₁₋₆ alquilo sustituido con 0 - 5 Rᵉ, C₂₋₆ alquenilo sustituido con 0 - 5 Rᵉ, C₂₋₆ alquinilo sustituido con 0 - 5 Rᵉ, -(CH₂)ₙ-C₃₋₁₀ carbociclilo sustituido con 0 - 5 Rᵉ y -(CH₂)ₙ-heterociclilo sustituido con 0 - 5 Rᵉ; Rᶜ, en cada caso, se selecciona independientemente C₁₋₆ alquilo sustituido con 0 - 5 Rᵉ, C₂₋₆ alquenilo sustituido con 0 - 5 Rᵉ, C₂₋₆ alquinilo sustituido con 0 - 5 Rᵉ, C₃₋₆ carbociclilo y heterociclilo; Rᵈ, en cada caso, se selecciona independientemente de H y C₁₋₄ alquilo sustituido con 0 - 5 Rᵉ; Rᵉ, en cada caso, se selecciona independientemente C₁₋₆ alquilo sustituido con 0 - 5 Rᶠ, C₂₋₆ alquenilo, C₂₋₆ alquinilo, -(CH₂)ₙ-C₃₋₆ cicloalquilo, -(CH₂)ₙ-C₄₋₆ heterociclilo, -(CH₂)ₙ-arilo, -(CH₂)ₙ-heteroarilo, F, Cl, Br, CN, NO₂, =O, CO₂H, -(CH₂)ₙORᶠ, S(O)ₚRᶠ, C(=O)NRᶠRᶠ, NRᶠC(=O)ₚRᶠ, S(O)ₚNRᶠRᶠ, NRᶠS(O)ₚRᶠ, NRᶠC(=O)ORᶠ, OC(=O)NRᶠRᶠ y -(CH₂)ₙNRᶠRᶠ; Rᶠ, en cada caso, se selecciona independientemente de H, F, Cl, Br, CN, OH, C₁₋₅ alquilo (de manera óptima, sustituido con halógeno y OH), C₃₋₆ cicloalquilo y fenilo, o Rᶠ y Rᶠ, junto con el átomo de nitrógeno al que están unidos, forman un anillo heterocíclico opcionalmente sustituido con C₁₋₄ alquilo; n se selecciona independientemente de 0, 1, 2 y 3; r se selecciona independientemente de 0, 1, 2 y 3; y p, en cada caso, se selecciona independientemente de 0, 1 y 2.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562170215P | 2015-06-03 | 2015-06-03 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR104884A1 true AR104884A1 (es) | 2017-08-23 |
Family
ID=56131647
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP160101639A AR104884A1 (es) | 2015-06-03 | 2016-06-02 | Compuestos de 4-hidroxi-3-(heteroaril)piridin-2-ona como agonistas de apj |
Country Status (36)
| Country | Link |
|---|---|
| US (3) | US10011594B2 (es) |
| EP (2) | EP3530660A1 (es) |
| JP (2) | JP6483288B2 (es) |
| KR (1) | KR102066336B1 (es) |
| CN (1) | CN107922401B (es) |
| AR (1) | AR104884A1 (es) |
| AU (1) | AU2016270903B2 (es) |
| CA (1) | CA2988147C (es) |
| CL (1) | CL2017003055A1 (es) |
| CO (1) | CO2017013229A2 (es) |
| CY (1) | CY1121938T1 (es) |
| DK (1) | DK3303330T3 (es) |
| EA (1) | EA034912B1 (es) |
| ES (1) | ES2739526T3 (es) |
| HK (1) | HK1247915B (es) |
| HR (1) | HRP20191327T1 (es) |
| HU (1) | HUE045546T2 (es) |
| IL (1) | IL255951B (es) |
| LT (1) | LT3303330T (es) |
| MA (1) | MA41562B1 (es) |
| ME (1) | ME03474B (es) |
| MX (1) | MX378998B (es) |
| MY (1) | MY189453A (es) |
| NZ (1) | NZ738563A (es) |
| PE (1) | PE20180506A1 (es) |
| PH (1) | PH12017502158B1 (es) |
| PL (1) | PL3303330T3 (es) |
| PT (1) | PT3303330T (es) |
| RS (1) | RS59220B1 (es) |
| SI (1) | SI3303330T1 (es) |
| SM (1) | SMT201900427T1 (es) |
| TN (1) | TN2017000503A1 (es) |
| TW (1) | TWI672299B (es) |
| UY (1) | UY36705A (es) |
| WO (1) | WO2016196771A1 (es) |
| ZA (1) | ZA201708191B (es) |
Families Citing this family (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2985542C (en) | 2015-05-20 | 2023-10-10 | Amgen Inc. | Triazole agonists of the apj receptor |
| RS59220B1 (sr) * | 2015-06-03 | 2019-10-31 | Bristol Myers Squibb Co | 4-hidroksi-3-(heteroaril)piridin-2-on apj agonisti za primenu u lečenju kardiovaskularnih poremećaja |
| SG10201908839QA (en) | 2015-10-14 | 2019-10-30 | Bristol Myers Squibb Co | 2,4-dihydroxy-nicotinamides as apj agonists |
| KR102678264B1 (ko) | 2015-12-04 | 2024-06-24 | 브리스톨-마이어스 스큅 컴퍼니 | 아펠린 수용체 효능제 및 사용 방법 |
| JP6948322B2 (ja) * | 2015-12-16 | 2021-10-13 | ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company | Apj受容体のapjアゴニストとしてのヘテロアリールヒドロキシピリミジノン |
| JP6716711B2 (ja) | 2016-03-24 | 2020-07-01 | ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company | Apjアゴニストとしての6−ヒドロキシ−4−オキソ−1,4−ジヒドロピリミジン−5−カルボキシアミド |
| WO2017192485A1 (en) | 2016-05-03 | 2017-11-09 | Amgen Inc. | Heterocyclic triazole compounds as agonists of the apj receptor |
| KR102384668B1 (ko) | 2016-06-14 | 2022-04-07 | 브리스톨-마이어스 스큅 컴퍼니 | Apj 효능제로서의 6-히드록시-5-(페닐/헤테로아릴술포닐)피리미딘-4(1h)-온 |
| EP3468952B1 (en) * | 2016-06-14 | 2020-11-25 | 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 |
| US11191762B2 (en) | 2016-11-16 | 2021-12-07 | Amgen Inc. | Alkyl substituted triazole compounds as agonists of the APJ Receptor |
| US10689367B2 (en) | 2016-11-16 | 2020-06-23 | Amgen Inc. | Triazole pyridyl compounds as agonists of the APJ receptor |
| WO2018093579A1 (en) | 2016-11-16 | 2018-05-24 | Amgen Inc. | Triazole phenyl 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 |
| WO2018097944A1 (en) | 2016-11-16 | 2018-05-31 | Amgen Inc. | Triazole furan compounds as agonists of the apj receptor |
| EP3541805B1 (en) | 2016-11-16 | 2020-10-14 | Amgen Inc. | Heteroaryl-substituted triazoles as apj receptor agonists |
| WO2018165520A1 (en) | 2017-03-10 | 2018-09-13 | Vps-3, Inc. | Metalloenzyme inhibitor compounds |
| MA50509A (fr) | 2017-11-03 | 2021-06-02 | Amgen Inc | Agonistes de triazole fusionnés du récepteur apj |
| MA52487A (fr) | 2018-05-01 | 2021-03-10 | Amgen Inc | Pyrimidinones substituées en tant qu'agonistes du récepteur apj |
| CN109704980B (zh) * | 2019-02-16 | 2022-05-13 | 安徽大学 | 一种(z)-3-氨基-2-(2-氟-3-甲氧基苯基)-2-丁烯酸乙酯的制备方法 |
| CN109704981B (zh) * | 2019-02-16 | 2022-01-28 | 安徽诺全药业有限公司 | 取代合成(z)-3-氨基-2-(2-氟-3-甲氧基苯基)-2-丁烯酸乙酯的方法 |
| CN109734616B (zh) * | 2019-02-16 | 2022-05-13 | 安徽诺全药业有限公司 | 两步法合成(z)-3-氨基-2-(2-氟-3-甲氧基苯基)-2-丁烯酸乙酯的方法 |
| CN114727974A (zh) | 2019-07-30 | 2022-07-08 | 艾科尼佐治疗股份有限公司 | Hdac6抑制剂及其用途 |
| CN120813365A (zh) | 2023-01-03 | 2025-10-17 | 百爱及生物医药公司 | 爱帕琳肽受体激动剂和glp-1受体激动剂的组合疗法用于治疗与体重增加相关的疾病或病况 |
| WO2025213190A1 (en) | 2024-04-05 | 2025-10-09 | BioAge Labs, Inc. | Methods of treating a disease or condition associated with weight gain |
| WO2025251084A1 (en) | 2024-05-31 | 2025-12-04 | BioAge Labs, Inc. | Methods of treating a disease or condition associated with weight gain |
Family Cites Families (73)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US1001159A (en) | 1910-07-25 | 1911-08-22 | Elizabeth Nielsen | Skirt-gage. |
| GB1472257A (en) | 1973-09-10 | 1977-05-04 | Christiaens Sa A | Derivative of 4-hydroxy-5-azacoumarin |
| US4866182A (en) | 1988-02-18 | 1989-09-12 | Merrell Dow Pharmaceuticals Inc. | Cardiotonic alkanoyl and aroyl oxazolones |
| US5338740A (en) | 1993-07-13 | 1994-08-16 | Pfizer Inc. | Angiotensin II receptor antagonists |
| JP3795305B2 (ja) | 1999-07-19 | 2006-07-12 | 田辺製薬株式会社 | 医薬組成物 |
| KR100838447B1 (ko) | 2001-02-21 | 2008-06-16 | 아스트라제네카 아베 | 헤테로폴리시클릭 화합물 및 대사향성 글루타메이트수용체 길항제로서의 그의 용도 |
| HRP20030751A2 (en) | 2001-03-28 | 2005-08-31 | Pfizer Inc. | N-phenpropylcyclopentyl-substituted glutaramide derivatives as nep inhibitors for fsad |
| WO2003020719A1 (en) | 2001-09-03 | 2003-03-13 | Takeda Chemical Industries, Ltd. | 1,3-benzothiazinone derivatives and use thereof |
| JP2005170790A (ja) | 2002-01-09 | 2005-06-30 | Ajinomoto Co Inc | N−アルキルスルフォニル置換アミド誘導体 |
| JP2005162612A (ja) | 2002-01-09 | 2005-06-23 | Ajinomoto Co Inc | アシルスルホンアミド誘導体 |
| ES2334990T3 (es) * | 2002-02-14 | 2010-03-18 | Pharmacia Corporation | Piridinonas sustituidas como moduladores de p38 map quinasa. |
| US20040147561A1 (en) * | 2002-12-27 | 2004-07-29 | Wenge Zhong | Pyrid-2-one derivatives and methods of use |
| WO2005004818A2 (en) | 2003-07-09 | 2005-01-20 | Imclone Systems Incorporated | Heterocyclic compounds and their use as anticancer agents |
| US20060004001A1 (en) | 2004-02-27 | 2006-01-05 | Merz Pharma Gmbh & Co., Kgaa | Tetrahydroquinolones and their use as modulators of metabotropic glutamate receptors |
| PE20060285A1 (es) * | 2004-03-30 | 2006-05-08 | Aventis Pharma Inc | Piridonas sustituidas como inhibidores de pol(adp-ribosa)-polimerasa (parp) |
| JP4777974B2 (ja) | 2004-04-01 | 2011-09-21 | イーライ リリー アンド カンパニー | ヒスタミンh3受容体作用物質、製剤および治療的使用 |
| NZ552187A (en) | 2004-06-18 | 2010-08-27 | Millennium Pharm Inc | Thiophene-2-carboxamide derivatives |
| JP4982367B2 (ja) | 2004-07-26 | 2012-07-25 | イーライ リリー アンド カンパニー | ヒスタミンh3受容体薬剤としてのオキサゾール誘導体、製造及び治療的使用 |
| EP1655283A1 (en) | 2004-11-08 | 2006-05-10 | Evotec OAI AG | 11beta-HSD1 Inhibitors |
| JP2008540626A (ja) * | 2005-05-19 | 2008-11-20 | アステックス、セラピューティックス、リミテッド | 医薬化合物 |
| WO2007023242A1 (en) | 2005-08-24 | 2007-03-01 | Merz Pharma Gmbh & Co. Kgaa | Tetrahydroquinolinones and their use as modulators of metabotropic glutamate receptors |
| EA018128B1 (ru) | 2006-01-23 | 2013-05-30 | Амген Инк. | Модуляторы аурора киназы, способы их получения и их применение |
| JP2007314516A (ja) | 2006-04-25 | 2007-12-06 | Daiichi Sankyo Co Ltd | 2以上の置換基を有するベンゼン化合物を含有する医薬 |
| CN101522623B (zh) | 2006-08-03 | 2013-06-12 | 塔夫茨大学信托人 | 无潮红烟酸类似物和其使用方法 |
| WO2008019090A2 (en) | 2006-08-04 | 2008-02-14 | Praecis Pharmaceuticals Incorporated | Agonists of the sphingosine-1-phosphate receptor |
| EP1894924A1 (en) | 2006-08-29 | 2008-03-05 | Phenex Pharmaceuticals AG | Heterocyclic FXR binding compounds |
| AU2007329512A1 (en) | 2006-12-01 | 2008-06-12 | Novartis Ag | Inhibitors of protein tyrosine phosphatase for the promotion of physiological cardiac hypertrophy |
| CA2682019C (en) | 2007-03-28 | 2016-08-09 | Neurosearch A/S | Purinyl derivatives and their use as potassium channel modulators |
| AU2008326309C1 (en) * | 2007-11-21 | 2015-03-12 | Decode Genetics Ehf | Biaryl PDE4 inhibitors for treating pulmonary and cardiovascular disorders |
| RU2010135524A (ru) | 2008-01-25 | 2012-02-27 | Торрент Фармасьютикалз Лтд. (In) | Фармацевтические комбинации |
| CN102046179B (zh) | 2008-04-09 | 2015-01-14 | 英菲尼提制药公司 | 脂肪酸酰胺水解酶抑制剂 |
| CN102047061A (zh) | 2008-05-30 | 2011-05-04 | 福斯特韦勒能源股份公司 | 通过氧化燃料燃烧发电的方法和系统 |
| BRPI0914942A2 (pt) | 2008-06-30 | 2015-08-11 | Cylene Pharmaceuticals Inc | Compostos de oxindol |
| JP5535931B2 (ja) | 2008-10-27 | 2014-07-02 | 武田薬品工業株式会社 | 二環性化合物 |
| CA2742528A1 (en) * | 2008-11-04 | 2010-05-14 | Anchor Therapeutics, Inc. | Apj receptor compounds |
| KR20120068947A (ko) | 2009-09-24 | 2012-06-27 | 에프. 호프만-라 로슈 아게 | Crac 조절제로서의 인돌 유도체 |
| CN102510864A (zh) | 2009-09-24 | 2012-06-20 | 弗·哈夫曼-拉罗切有限公司 | 抗病毒杂环化合物 |
| US8609663B2 (en) | 2009-11-18 | 2013-12-17 | University Of Massachusetts | Compounds for modulating TLR2 |
| JP2013515000A (ja) | 2009-12-18 | 2013-05-02 | アクティベサイト ファーマシューティカルズ インコーポレイティッド | 血漿カリクレインの阻害薬のプロドラッグ |
| CN102241621A (zh) | 2010-05-11 | 2011-11-16 | 江苏恒瑞医药股份有限公司 | 5,5-双取代-2-亚氨基吡咯烷类衍生物、其制备方法及其在医药上的应用 |
| CN102906074A (zh) | 2010-05-24 | 2013-01-30 | 东亚荣养株式会社 | 稠合咪唑衍生物 |
| WO2012040532A1 (en) * | 2010-09-24 | 2012-03-29 | Bristol-Myers Squibb Company | Substituted oxadiazole compounds and their use as s1p1 agonists |
| JPWO2012074022A1 (ja) | 2010-12-01 | 2014-05-19 | 旭硝子株式会社 | イリジウムカチオン錯体および発光組成物 |
| US20140057953A1 (en) | 2011-03-03 | 2014-02-27 | Rolf Hartmann | Biaryl derivatives as selective 17beta-hydroxysteroid dehydrogenase type 2 inhibitors |
| US8691861B2 (en) | 2011-04-13 | 2014-04-08 | Activesite Pharmaceuticals, Inc. | Prodrugs of inhibitors of plasma kallikrein |
| EP2709609B1 (en) | 2011-05-17 | 2017-10-04 | Shionogi & Co., Ltd. | Heterocyclic compounds |
| EP2794601B1 (en) | 2011-12-23 | 2019-02-20 | Basf Se | Isothiazoline compounds for combating invertebrate pests |
| WO2013164769A1 (en) * | 2012-05-02 | 2013-11-07 | Lupin Limited | Substituted pyridine compounds as crac modulators |
| WO2013167633A1 (en) | 2012-05-09 | 2013-11-14 | Basf Se | Acrylamide compounds for combating invertebrate pests |
| CN107569483B (zh) | 2012-06-08 | 2021-09-17 | 高等教育联邦系统-匹兹堡大学 | 选自苄星青霉素化合物等的化合物在制备用于治疗炎症疾病的药物中的用途 |
| WO2014006045A1 (en) | 2012-07-02 | 2014-01-09 | Max-Delbrück-Centrum für Molekulare Medizin | Psoralen derivatives for preventing or treating heart failure or cardiac hypertrophy |
| CN103570625A (zh) | 2012-07-19 | 2014-02-12 | 南京英派药业有限公司 | N-(3-杂芳基芳基)-4-芳基芳基甲酰胺和类似物作为Hedgehog通路抑制剂及其应用 |
| WO2014031928A2 (en) | 2012-08-24 | 2014-02-27 | Philip Jones | Heterocyclic modulators of hif activity for treatment of disease |
| DK2897939T3 (en) * | 2012-09-21 | 2017-05-08 | Sanofi Sa | BENZOIMIDAZOLCARBOXYL ACID AMIDE DERIVATIVES FOR THE TREATMENT OF METABOLIC OR CARDIOVASCULAR DISEASES |
| US10035790B2 (en) | 2012-10-19 | 2018-07-31 | Exelixis, Inc. | RORγ modulators |
| US10201623B2 (en) | 2013-03-15 | 2019-02-12 | Memorial Sloan Kettering Cancer Center | HSP90-targeted cardiac imaging and therapy |
| WO2015017305A1 (en) | 2013-07-31 | 2015-02-05 | Merck Sharp & Dohme Corp | Inhibitors of the renal outer medullary potassium channel |
| JP6199197B2 (ja) | 2014-02-07 | 2017-09-20 | 花王株式会社 | ポリオキシアルキレンアルキルエーテルカルボン酸塩の製造方法 |
| JP2017071553A (ja) | 2014-02-25 | 2017-04-13 | 味の素株式会社 | ヘテロ原子−メチレン−ヘテロ環構造を有する新規化合物 |
| PE20170186A1 (es) | 2014-03-20 | 2017-04-01 | Bayer Pharma AG | Nuevos compuestos |
| WO2015191630A1 (en) | 2014-06-10 | 2015-12-17 | Sanford-Burnham Medical Research Institute | Metabotropic glutamate receptor negative allosteric modulators (nams) and uses thereof |
| CA2985542C (en) | 2015-05-20 | 2023-10-10 | Amgen Inc. | Triazole agonists of the apj receptor |
| RS59220B1 (sr) * | 2015-06-03 | 2019-10-31 | Bristol Myers Squibb Co | 4-hidroksi-3-(heteroaril)piridin-2-on apj agonisti za primenu u lečenju kardiovaskularnih poremećaja |
| KR101711744B1 (ko) | 2015-07-16 | 2017-03-02 | 경희대학교 산학협력단 | 옥사디아졸 유도체, 이의 제조방법 및 이를 포함하는 전자수송층 |
| SG10201908839QA (en) | 2015-10-14 | 2019-10-30 | Bristol Myers Squibb Co | 2,4-dihydroxy-nicotinamides as apj agonists |
| WO2017091513A1 (en) | 2015-11-24 | 2017-06-01 | Daiichi Sankyo Company, Limited | Novel azole derivatives as apelin receptor agonist |
| KR102678264B1 (ko) | 2015-12-04 | 2024-06-24 | 브리스톨-마이어스 스큅 컴퍼니 | 아펠린 수용체 효능제 및 사용 방법 |
| PE20190258A1 (es) | 2015-12-09 | 2019-02-25 | Res Triangle Inst | Antagonistas del receptor de la apelina (apj) mejorados y usos de los mismos |
| JP6948322B2 (ja) | 2015-12-16 | 2021-10-13 | ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company | Apj受容体のapjアゴニストとしてのヘテロアリールヒドロキシピリミジノン |
| JP6716711B2 (ja) | 2016-03-24 | 2020-07-01 | ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company | Apjアゴニストとしての6−ヒドロキシ−4−オキソ−1,4−ジヒドロピリミジン−5−カルボキシアミド |
| KR102384668B1 (ko) | 2016-06-14 | 2022-04-07 | 브리스톨-마이어스 스큅 컴퍼니 | Apj 효능제로서의 6-히드록시-5-(페닐/헤테로아릴술포닐)피리미딘-4(1h)-온 |
| EP3468952B1 (en) | 2016-06-14 | 2020-11-25 | 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 |
-
2016
- 2016-06-02 RS RSP20190961 patent/RS59220B1/sr unknown
- 2016-06-02 NZ NZ73856316A patent/NZ738563A/en unknown
- 2016-06-02 US US15/171,276 patent/US10011594B2/en active Active
- 2016-06-02 PH PH1/2017/502158A patent/PH12017502158B1/en unknown
- 2016-06-02 DK DK16729454.5T patent/DK3303330T3/da active
- 2016-06-02 HK HK18107278.8A patent/HK1247915B/en unknown
- 2016-06-02 MA MA41562A patent/MA41562B1/fr unknown
- 2016-06-02 EP EP19168724.3A patent/EP3530660A1/en not_active Withdrawn
- 2016-06-02 AU AU2016270903A patent/AU2016270903B2/en active Active
- 2016-06-02 MY MYPI2017704612A patent/MY189453A/en unknown
- 2016-06-02 HR HRP20191327 patent/HRP20191327T1/hr unknown
- 2016-06-02 TN TNP/2017/000503A patent/TN2017000503A1/en unknown
- 2016-06-02 KR KR1020177037657A patent/KR102066336B1/ko active Active
- 2016-06-02 UY UY0001036705A patent/UY36705A/es unknown
- 2016-06-02 PT PT16729454T patent/PT3303330T/pt unknown
- 2016-06-02 LT LTEP16729454.5T patent/LT3303330T/lt unknown
- 2016-06-02 SI SI201630316T patent/SI3303330T1/sl unknown
- 2016-06-02 JP JP2017562603A patent/JP6483288B2/ja active Active
- 2016-06-02 CN CN201680045336.7A patent/CN107922401B/zh active Active
- 2016-06-02 EP EP16729454.5A patent/EP3303330B1/en active Active
- 2016-06-02 ME MEP-2019-211A patent/ME03474B/me unknown
- 2016-06-02 SM SM20190427T patent/SMT201900427T1/it unknown
- 2016-06-02 TW TW105117468A patent/TWI672299B/zh active
- 2016-06-02 WO PCT/US2016/035482 patent/WO2016196771A1/en not_active Ceased
- 2016-06-02 MX MX2017014956A patent/MX378998B/es unknown
- 2016-06-02 CA CA2988147A patent/CA2988147C/en active Active
- 2016-06-02 PE PE2017002482A patent/PE20180506A1/es unknown
- 2016-06-02 ES ES16729454T patent/ES2739526T3/es active Active
- 2016-06-02 PL PL16729454T patent/PL3303330T3/pl unknown
- 2016-06-02 HU HUE16729454A patent/HUE045546T2/hu unknown
- 2016-06-02 AR ARP160101639A patent/AR104884A1/es unknown
- 2016-06-02 EA EA201792548A patent/EA034912B1/ru not_active IP Right Cessation
-
2017
- 2017-11-27 IL IL255951A patent/IL255951B/en active IP Right Grant
- 2017-11-30 CL CL2017003055A patent/CL2017003055A1/es unknown
- 2017-12-01 ZA ZA2017/08191A patent/ZA201708191B/en unknown
- 2017-12-21 CO CONC2017/0013229A patent/CO2017013229A2/es unknown
-
2018
- 2018-05-29 US US15/990,855 patent/US10336739B2/en active Active
-
2019
- 2019-02-13 JP JP2019023478A patent/JP2019094345A/ja active Pending
- 2019-05-14 US US16/411,221 patent/US20190263791A1/en not_active Abandoned
- 2019-07-29 CY CY20191100803T patent/CY1121938T1/el unknown
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AR104884A1 (es) | Compuestos de 4-hidroxi-3-(heteroaril)piridin-2-ona como agonistas de apj | |
| AR107061A1 (es) | Heteroarilhidroxipirimidinonas como agonistas del receptor de apj | |
| AR106948A1 (es) | Agonistas del receptor de apelina y método de uso | |
| AR110405A1 (es) | Compuestos | |
| AR107973A1 (es) | 6-hidroxi-4-oxo-1,4-dihidropirimidin-5-carboxamidas como agonista de apj | |
| AR103990A1 (es) | Ureas cíclicas como inhibidoras de rock | |
| AR096788A1 (es) | Compuestos tricíclicos de carboxamida como inhibidores potentes de rock | |
| AR099379A1 (es) | Compuestos tricíclicos como agentes antineoplásicos | |
| AR092349A1 (es) | Imidazotriazincarbonitrilos utiles como inhibidores de quinasa | |
| AR103064A1 (es) | Compuestos moduladores de fxr (nr1h4) | |
| AR104176A1 (es) | Inhibidores de ido (indolamina-2,3-dioxigenasa) | |
| AR117617A1 (es) | Compuestos de sulfonilurea como inhibidores de la actividad de interleuquina 1 | |
| AR100645A1 (es) | Derivados de pirazolo-pirimidina | |
| AR102177A1 (es) | Compuestos de heteroarilo como inhibidores de btk y usos de los mismos | |
| AR088829A1 (es) | DERIVADOS DE CICLOHEXILAMINA QUE TIENEN ACTIVIDAD COMO AGONISTAS ADRENERGICOS b2 Y COMO ANTAGONISTAS MUSCARINICOS M3 | |
| AR077695A1 (es) | Derivados de pirimidina como inhibidores del factor ixa | |
| AR097082A1 (es) | Compuestos terapéuticamente activos y sus métodos de uso | |
| AR103232A1 (es) | ANTAGONISTAS DE TGFbR | |
| AR107321A1 (es) | Compuestos antiproliferativos, y sus composiciones farmacéuticas y usos | |
| AR090557A1 (es) | DERIVADOS IMIDAZOLICOS AGONISTAS ADRENERGICOS a2 | |
| AR119376A1 (es) | Compuestos heterocíclicos | |
| AR101132A1 (es) | Derivados de pirazina agonistas del gpr40 para el tratamiento de la diabetes tipo ii | |
| AR101589A1 (es) | Derivados de iminonitrilo | |
| AR102825A1 (es) | Derivados heterocíclicos de amida activos como plaguicidas con sustituyentes que contienen azufre | |
| AR100439A1 (es) | Derivados de carboxamida |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |