MX367525B - Derivados de ácido bisfenil-butanoico fosfónico sustituido como inhibidores de la endopeptidasa neutra (nep). - Google Patents
Derivados de ácido bisfenil-butanoico fosfónico sustituido como inhibidores de la endopeptidasa neutra (nep).Info
- Publication number
- MX367525B MX367525B MX2015010433A MX2015010433A MX367525B MX 367525 B MX367525 B MX 367525B MX 2015010433 A MX2015010433 A MX 2015010433A MX 2015010433 A MX2015010433 A MX 2015010433A MX 367525 B MX367525 B MX 367525B
- Authority
- MX
- Mexico
- Prior art keywords
- nep
- inhibitors
- acid derivatives
- phosphonic acid
- neutral endopeptidase
- Prior art date
Links
- 102000003729 Neprilysin Human genes 0.000 title 1
- 108090000028 Neprilysin Proteins 0.000 title 1
- 229940042400 direct acting antivirals phosphonic acid derivative Drugs 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 150000003007 phosphonic acid derivatives Chemical class 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 4
- 239000013543 active substance Substances 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 230000001225 therapeutic effect Effects 0.000 abstract 1
Classifications
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- 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
- C07F9/28—Phosphorus compounds with one or more P—C bonds
- C07F9/38—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
- C07F9/3804—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)] not used, see subgroups
- C07F9/3808—Acyclic saturated acids which can have further substituents on alkyl
-
- 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
- A61K31/662—Phosphorus acids or esters thereof having P—C bonds, e.g. foscarnet, trichlorfon
-
- 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
- A61K31/665—Phosphorus compounds having oxygen as a ring hetero atom, e.g. fosfomycin
-
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- 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
-
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- 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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- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
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- 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
- C07F9/553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
- C07F9/572—Five-membered rings
-
- 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
- C07F9/553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
- C07F9/576—Six-membered rings
- C07F9/59—Hydrogenated pyridine rings
-
- 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
- C07F9/655—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having oxygen atoms, with or without sulfur, selenium, or tellurium atoms, as the only ring hetero atoms
- C07F9/65515—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having oxygen atoms, with or without sulfur, selenium, or tellurium atoms, as the only ring hetero atoms the oxygen atom being part of a five-membered ring
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Diabetes (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Cardiology (AREA)
- Hematology (AREA)
- Neurology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pain & Pain Management (AREA)
- Ophthalmology & Optometry (AREA)
- Obesity (AREA)
- Pulmonology (AREA)
- Rheumatology (AREA)
- Oncology (AREA)
- Endocrinology (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Dermatology (AREA)
- Urology & Nephrology (AREA)
- Child & Adolescent Psychology (AREA)
- Communicable Diseases (AREA)
- Emergency Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
La presente invención proporciona un compuesto de la fórmula (I); (ver Fórmula) o una sal farmacéuticamente aceptable del mismo, en donde R1, R2 y R3 se definen en la presente. La invención también se refiere a un método para la elaboración de los compuestos de la invención, y a sus usos terapéuticos. La presente invención proporciona además una composición farmacéutica de los compuestos de la invención, y una combinación de los agentes farmacológicamente activos y un compuesto de la invención.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361764679P | 2013-02-14 | 2013-02-14 | |
| PCT/US2014/015980 WO2014126979A1 (en) | 2013-02-14 | 2014-02-12 | Substituted bisphenyl butanoic phosphonic acid derivatives as nep (neutral endopeptidase) inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| MX2015010433A MX2015010433A (es) | 2015-10-05 |
| MX367525B true MX367525B (es) | 2019-08-26 |
Family
ID=50193599
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2015010433A MX367525B (es) | 2013-02-14 | 2014-02-12 | Derivados de ácido bisfenil-butanoico fosfónico sustituido como inhibidores de la endopeptidasa neutra (nep). |
Country Status (37)
| Country | Link |
|---|---|
| US (3) | US9163040B2 (es) |
| EP (1) | EP2956464B1 (es) |
| JP (1) | JP6295277B2 (es) |
| KR (1) | KR20150119109A (es) |
| CN (1) | CN105073762B (es) |
| AP (1) | AP2015008621A0 (es) |
| AR (1) | AR094790A1 (es) |
| AU (1) | AU2014216424B2 (es) |
| BR (1) | BR112015019369A2 (es) |
| CA (1) | CA2900027A1 (es) |
| CR (1) | CR20150419A (es) |
| CU (1) | CU24330B1 (es) |
| CY (1) | CY1120378T1 (es) |
| DK (1) | DK2956464T3 (es) |
| EA (1) | EA028583B1 (es) |
| ES (1) | ES2675216T3 (es) |
| HK (1) | HK1212704A1 (es) |
| HR (1) | HRP20180958T1 (es) |
| HU (1) | HUE038248T2 (es) |
| IL (1) | IL240336A0 (es) |
| LT (1) | LT2956464T (es) |
| MA (1) | MA38330B1 (es) |
| MX (1) | MX367525B (es) |
| NZ (1) | NZ710574A (es) |
| PE (1) | PE20151666A1 (es) |
| PH (1) | PH12015501752B1 (es) |
| PL (1) | PL2956464T3 (es) |
| PT (1) | PT2956464T (es) |
| RS (1) | RS57358B1 (es) |
| SG (1) | SG11201506018PA (es) |
| SI (1) | SI2956464T1 (es) |
| TN (1) | TN2015000324A1 (es) |
| TR (1) | TR201808541T4 (es) |
| TW (1) | TWI636057B (es) |
| UY (1) | UY35325A (es) |
| WO (1) | WO2014126979A1 (es) |
| ZA (1) | ZA201505490B (es) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HUE038248T2 (hu) | 2013-02-14 | 2018-10-29 | Novartis Ag | Helyettesített biszfenil-bután-foszfonsav származékok, mint NEP (semleges endopeptidáz) inhibitorok |
| CN106397249A (zh) * | 2015-08-03 | 2017-02-15 | 深圳信立泰药业股份有限公司 | 一种高稳定性lcz696结晶粉末及其制备方法 |
| CN105748420B (zh) * | 2016-03-04 | 2018-11-06 | 山东省药学科学院 | 一种治疗心力衰竭的lcz696缓释骨架片的制备方法 |
| CN107764910B (zh) * | 2017-09-05 | 2020-02-07 | 华侨大学 | 一种沙库比曲缬沙坦三钠半五水合物胶囊有效成分的含量测定方法 |
| UY38072A (es) | 2018-02-07 | 2019-10-01 | Novartis Ag | Compuestos derivados de éster butanoico sustituido con bisfenilo como inhibidores de nep, composiciones y combinaciones de los mismos |
| EP3887363A1 (en) | 2018-11-27 | 2021-10-06 | Novartis AG | Cyclic pentamer compounds as proprotein convertase subtilisin/kexin type 9 (pcsk9) inhibitors for the treatment of metabolic disorder |
| WO2020110011A1 (en) | 2018-11-27 | 2020-06-04 | Novartis Ag | Cyclic peptides as proprotein convertase subtilisin/kexin type 9 (pcsk9) inhibitors for the treatment of metabolic disorders |
| UY38485A (es) | 2018-11-27 | 2020-06-30 | Novartis Ag | Compuestos tetrámeros cíclicos como inhibidores de proproteína convertasa subtilisina/kexina tipo 9 (pcsk9), método de tratamiento, uso y su preparación |
| IL301285A (en) | 2020-09-10 | 2023-05-01 | Precirix N V | A portion of an antibody against FAP |
| TW202333563A (zh) | 2021-11-12 | 2023-09-01 | 瑞士商諾華公司 | 用於治療疾病或障礙之二胺基環戊基吡啶衍生物 |
| WO2023203135A1 (en) | 2022-04-22 | 2023-10-26 | Precirix N.V. | Improved radiolabelled antibody |
| AU2023264245A1 (en) | 2022-05-02 | 2024-12-19 | Precirix N.V. | Pre-targeting |
Family Cites Families (145)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS5262709A (en) | 1975-11-20 | 1977-05-24 | Nisshin Spinning | Cylindrical impellers |
| DE2947140A1 (de) | 1978-11-25 | 1980-06-12 | Nippon Kayaku Kk | Verfahren zur herstellung von threo-3-amino-2-hydroxybutanoyl- aminoessigsaeure |
| DE2951135A1 (de) | 1979-12-19 | 1981-06-25 | Hoechst Ag, 6230 Frankfurt | Sulfonylharnstoffe, verfahren zu ihrer herstellung, pharmazeutische praeparate auf basis dieser verbindungen und ihre verwendung |
| DE3162404D1 (en) | 1980-04-11 | 1984-04-05 | Wellcome Found | Pharmaceutical amides, and preparation, formulations and use thereof |
| PT72878B (en) | 1980-04-24 | 1983-03-29 | Merck & Co Inc | Process for preparing mannich-base hydroxamic acid pro-drugs for the improved delivery of non-steroidal anti-inflammatory agents |
| US4610816A (en) | 1980-12-18 | 1986-09-09 | Schering Corporation | Substituted dipeptides as inhibitors of enkephalinases |
| US4721726A (en) | 1980-12-18 | 1988-01-26 | Schering Corporation | Substituted dipeptides as inhibitors of enkephalinases |
| JPS5865260A (ja) | 1981-10-13 | 1983-04-18 | Microbial Chem Res Found | ３−アミノ−２−ヒドロキシ−４−フエニル酪酸誘導体および医薬組成物 |
| FR2518088B1 (fr) | 1981-12-16 | 1987-11-27 | Roques Bernard | Nouveaux derives d'aminoacides, et leur application therapeutique |
| EP0103077B1 (en) | 1982-06-17 | 1988-05-18 | Schering Corporation | Substituted dipeptides, methods for their production, pharmaceutical compositions containing them, method for making such pharmaceutical compositions |
| US4617307A (en) | 1984-06-20 | 1986-10-14 | Ciba-Geigy Corporation | Substituted imidazo[1,5-A]pyridine derivatives as aromatase inhibitors |
| US4889861A (en) | 1982-12-21 | 1989-12-26 | Ciba-Geigy Corp. | Substituted imidazo[1,5-a]pyridine derivatives and other substituted bicyclic derivatives and their use as aromatase inhibitors |
| NZ206920A (en) | 1983-01-28 | 1986-10-08 | Schering Corp | Phosphorus-containing amide,urea or carbamate derivatives and pharmaceutical compositions |
| FI77669C (fi) | 1983-04-13 | 1989-04-10 | Ciba Geigy Ag | 20-spiroxaner och analoger, som innehaoller en oeppen ring e, foerfarande foer deras framstaellning samt dessa innehaollande farmaceutiska preparat. |
| EP0136883B1 (en) | 1983-10-03 | 1987-11-25 | E.R. Squibb & Sons, Inc. | Enkephalinase inhibitors |
| DE3347565A1 (de) | 1983-12-30 | 1985-07-11 | Thomae Gmbh Dr K | Neue phenylessigsaeurederivate, diese verbindungen enthaltende arzneimittel und verfahren zu ihrer herstellung |
| JPS60248659A (ja) | 1984-05-25 | 1985-12-09 | Microbial Chem Res Found | ３−〔ｎ−（メルカプトアシル）〕アミノ−４−アリ−ル酪酸誘導体及びそれを有効成分とする鎮痛剤 |
| JPS6354321A (ja) | 1985-03-27 | 1988-03-08 | Ajinomoto Co Inc | 血糖降下剤 |
| JPS6234630A (ja) | 1985-08-09 | 1987-02-14 | Kobe Steel Ltd | ライニング管およびその製造方法 |
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