PE20190735A1 - Derivados de naftiridinona y su uso en el tratamiento de la arritmia - Google Patents
Derivados de naftiridinona y su uso en el tratamiento de la arritmiaInfo
- Publication number
- PE20190735A1 PE20190735A1 PE2019000829A PE2019000829A PE20190735A1 PE 20190735 A1 PE20190735 A1 PE 20190735A1 PE 2019000829 A PE2019000829 A PE 2019000829A PE 2019000829 A PE2019000829 A PE 2019000829A PE 20190735 A1 PE20190735 A1 PE 20190735A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- 4alkyl
- optionally substituted
- compounds
- treatment
- Prior art date
Links
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 3
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 150000002367 halogens Chemical class 0.000 abstract 2
- -1 -CH2CN Chemical group 0.000 abstract 1
- DDDSGZFENQKDDY-UHFFFAOYSA-N 8-chloro-1-(2,6-dichlorophenyl)-5-(2,3-dihydroxypropoxy)-2-(hydroxymethyl)-1,6-naphthyridin-4-one Chemical compound ClC=1C=NC(=C2C(C=C(N(C=12)C1=C(C=CC=C1Cl)Cl)CO)=O)OCC(CO)O DDDSGZFENQKDDY-UHFFFAOYSA-N 0.000 abstract 1
- DDDSGZFENQKDDY-SNVBAGLBSA-N 8-chloro-1-(2,6-dichlorophenyl)-5-[(2R)-2,3-dihydroxypropoxy]-2-(hydroxymethyl)-1,6-naphthyridin-4-one Chemical compound ClC=1C=NC(=C2C(C=C(N(C=12)C1=C(C=CC=C1Cl)Cl)CO)=O)OC[C@@H](CO)O DDDSGZFENQKDDY-SNVBAGLBSA-N 0.000 abstract 1
- 206010003658 Atrial Fibrillation Diseases 0.000 abstract 1
- 125000002853 C1-C4 hydroxyalkyl group Chemical group 0.000 abstract 1
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract 1
- 208000016998 Conn syndrome Diseases 0.000 abstract 1
- 206010020772 Hypertension Diseases 0.000 abstract 1
- 206010003119 arrhythmia Diseases 0.000 abstract 1
- 230000000903 blocking effect Effects 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- 208000013846 primary aldosteronism Diseases 0.000 abstract 1
- 201000009395 primary hyperaldosteronism Diseases 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic 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
- C07D471/02—Heterocyclic 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
- C07D471/04—Ortho-condensed systems
-
- 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
- A61K31/4375—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 six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
-
- 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
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- 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
- A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
- A61K31/541—Non-condensed thiazines 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
- A61K31/66—Phosphorus compounds
- A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
-
- 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
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/06—Antiarrhythmics
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Se refiere a compuestos de Formula (I), donde: X2 es N, entre otros; X3 es CH o N; R1 es alquilo C1-4, -CH2CN, -CN, alcoxiC1-4alquiloC1-4, entre otros; R3 es -C(O)NH2; -C(O)[hidroxialquilC1-4, heterociclilo, entre otros; opcionalmente sustituido con uno o mas sustituyentes independientemente seleccionados entre OH e hidroxialquilo C1-C4, entre otros; heteroarilo de anillo de 5 o 6 miembros opcionalmente sustituidos con uno o mas alquilo C1-C4; R4 es H, halogeno, halo-alquiloC1-C4, alquilo C1-C4; R5 es alquinilo C2-C6, opcionalmente sustituido con OH o alquiloC1-4; R6 es halogeno, alquiloC1-4 o CN, o una sal farmaceuticamente aceptable del mismo. Son compuestos preferidos (R )-8-cloro-1-(2,6-diclorofenil)-5-(2,3-dihidroxipropoxi)-2-(hidroximetil)-1,6-naftiridin-4(1H)-ona; 8-cloro-1-(2,6-diclorofenil)-5-(2,3-dihidroxipropoxi)-2-(hidroximetil)-1,6-naftiridin-4(1H)-ona. Dichos compuestos son capaces de bloquear el canal de GIRK ¼ y utiles en el tratamiento, prevencion o mejoramiento de arritmia cardiaca, fibrilacion auricular, hiperaldosteronismo primario, hipertension, entre otros.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662410930P | 2016-10-21 | 2016-10-21 | |
| CN2016102928 | 2016-10-21 | ||
| US201662413292P | 2016-10-26 | 2016-10-26 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20190735A1 true PE20190735A1 (es) | 2019-05-23 |
Family
ID=60409317
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2019000829A PE20190735A1 (es) | 2016-10-21 | 2017-10-19 | Derivados de naftiridinona y su uso en el tratamiento de la arritmia |
Country Status (32)
| Country | Link |
|---|---|
| US (3) | US10266531B2 (es) |
| EP (2) | EP3529251B1 (es) |
| JP (1) | JP7030802B2 (es) |
| KR (1) | KR102540872B1 (es) |
| CN (1) | CN109843887B (es) |
| AU (2) | AU2017344489C1 (es) |
| CA (1) | CA3038624A1 (es) |
| CL (1) | CL2019001023A1 (es) |
| CO (1) | CO2019003894A2 (es) |
| CR (1) | CR20190201A (es) |
| CU (1) | CU24599B1 (es) |
| DO (1) | DOP2019000100A (es) |
| EC (1) | ECSP19026973A (es) |
| ES (1) | ES2934234T3 (es) |
| FI (1) | FI3529251T3 (es) |
| HR (1) | HRP20221516T1 (es) |
| HU (1) | HUE060882T2 (es) |
| IL (1) | IL266128B (es) |
| JO (1) | JOP20190086A1 (es) |
| LT (1) | LT3529251T (es) |
| MX (1) | MX390044B (es) |
| PE (1) | PE20190735A1 (es) |
| PH (1) | PH12019500849A1 (es) |
| PL (1) | PL3529251T3 (es) |
| PT (1) | PT3529251T (es) |
| RS (1) | RS63841B1 (es) |
| SA (1) | SA519401614B1 (es) |
| SG (1) | SG11201902529WA (es) |
| SI (1) | SI3529251T1 (es) |
| TW (1) | TWI759343B (es) |
| UY (1) | UY37445A (es) |
| WO (1) | WO2018073788A1 (es) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JOP20190086A1 (ar) | 2016-10-21 | 2019-04-18 | Novartis Ag | مشتقات نافثيريدينون جديدة واستخدامها في معالجة عدم انتظام ضربات القلب |
| PL3814347T3 (pl) | 2018-06-27 | 2023-07-24 | Bristol-Myers Squibb Company | Związki naftyrydynonu użyteczne jako aktywatory komórek t |
| WO2022074567A1 (en) * | 2020-10-06 | 2022-04-14 | Novartis Ag | Pharmaceutical compositions comprising naphthyridinone derivatives and their use in the treatment of arrhythmia |
| CN115677739B (zh) * | 2021-07-31 | 2025-09-30 | 华南理工大学 | 一种o,o-二氟化硼配合物的制备方法 |
| AR127698A1 (es) | 2021-11-23 | 2024-02-21 | Novartis Ag | Derivados de naftiridinona para el tratamiento de una enfermedad o un trastorno |
| EP4574830A4 (en) * | 2022-09-23 | 2025-11-26 | Guangzhou Vinnocent Pharmaceutical Ltd | PYRIDINE INHIBITOR, RINGED STEROID SYNTHETASE, ITS PREPARATION PROCESS AND ITS USE |
| US20240391941A1 (en) * | 2023-05-24 | 2024-11-28 | Novartis Ag | Naphthyridinone derivatives for the treatment of a disease or disorder |
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