AR070176A1 - Procesos de sintesis de inhibidores de nep, compuestos intermediarios y uso de los mismos en la sintesis - Google Patents
Procesos de sintesis de inhibidores de nep, compuestos intermediarios y uso de los mismos en la sintesisInfo
- Publication number
- AR070176A1 AR070176A1 ARP090100121A ARP090100121A AR070176A1 AR 070176 A1 AR070176 A1 AR 070176A1 AR P090100121 A ARP090100121 A AR P090100121A AR P090100121 A ARP090100121 A AR P090100121A AR 070176 A1 AR070176 A1 AR 070176A1
- Authority
- AR
- Argentina
- Prior art keywords
- salt
- formula
- compound
- cycle
- alkyl group
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 8
- 238000000034 method Methods 0.000 title abstract 5
- 239000003112 inhibitor Substances 0.000 title abstract 4
- 230000015572 biosynthetic process Effects 0.000 title abstract 3
- 238000003786 synthesis reaction Methods 0.000 title abstract 3
- 150000003839 salts Chemical class 0.000 abstract 5
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 4
- -1 alkali metal salt Chemical class 0.000 abstract 4
- 229910052757 nitrogen Inorganic materials 0.000 abstract 4
- 229910052783 alkali metal Inorganic materials 0.000 abstract 3
- 229910052784 alkaline earth metal Inorganic materials 0.000 abstract 3
- 125000000217 alkyl group Chemical group 0.000 abstract 3
- 150000001450 anions Chemical class 0.000 abstract 3
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 3
- 125000003118 aryl group Chemical group 0.000 abstract 3
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 abstract 2
- 239000002253 acid Substances 0.000 abstract 2
- 150000001340 alkali metals Chemical class 0.000 abstract 2
- 150000001342 alkaline earth metals Chemical class 0.000 abstract 2
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 abstract 2
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 2
- 125000005842 heteroatom Chemical group 0.000 abstract 2
- 239000001257 hydrogen Substances 0.000 abstract 2
- 229910052739 hydrogen Inorganic materials 0.000 abstract 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 2
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 abstract 2
- 229910052760 oxygen Inorganic materials 0.000 abstract 2
- 239000001301 oxygen Substances 0.000 abstract 2
- 125000006413 ring segment Chemical group 0.000 abstract 2
- 229920006395 saturated elastomer Polymers 0.000 abstract 2
- 229910052717 sulfur Inorganic materials 0.000 abstract 2
- 239000011593 sulfur Substances 0.000 abstract 2
- QGZKDVFQNNGYKY-UHFFFAOYSA-O Ammonium Chemical compound [NH4+] QGZKDVFQNNGYKY-UHFFFAOYSA-O 0.000 abstract 1
- LSNNMFCWUKXFEE-UHFFFAOYSA-M Bisulfite Chemical compound OS([O-])=O LSNNMFCWUKXFEE-UHFFFAOYSA-M 0.000 abstract 1
- GPWHDDKQSYOYBF-UHFFFAOYSA-N ac1l2u0q Chemical compound Br[Br-]Br GPWHDDKQSYOYBF-UHFFFAOYSA-N 0.000 abstract 1
- 150000004703 alkoxides Chemical class 0.000 abstract 1
- 150000008051 alkyl sulfates Chemical class 0.000 abstract 1
- 150000001412 amines Chemical class 0.000 abstract 1
- 150000003863 ammonium salts Chemical class 0.000 abstract 1
- 229910052787 antimony Inorganic materials 0.000 abstract 1
- 239000002585 base Substances 0.000 abstract 1
- 150000007942 carboxylates Chemical class 0.000 abstract 1
- 150000002148 esters Chemical class 0.000 abstract 1
- 150000004820 halides Chemical class 0.000 abstract 1
- 239000000543 intermediate Substances 0.000 abstract 1
- 239000002608 ionic liquid Substances 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- VLTRZXGMWDSKGL-UHFFFAOYSA-M perchlorate Inorganic materials [O-]Cl(=O)(=O)=O VLTRZXGMWDSKGL-UHFFFAOYSA-M 0.000 abstract 1
- VLTRZXGMWDSKGL-UHFFFAOYSA-N perchloric acid Chemical compound OCl(=O)(=O)=O VLTRZXGMWDSKGL-UHFFFAOYSA-N 0.000 abstract 1
- 238000002360 preparation method Methods 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
- C07D207/34—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two 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
- C07D207/36—Oxygen or sulfur atoms
- C07D207/38—2-Pyrrolones
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/10—Antioedematous agents; Diuretics
-
- 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
- A61P9/12—Antihypertensives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
- C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member 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
- C07D207/24—Oxygen or sulfur atoms
- C07D207/26—2-Pyrrolidones
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
- C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member 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
- C07D207/24—Oxygen or sulfur atoms
- C07D207/26—2-Pyrrolidones
- C07D207/263—2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
- C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member 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
- C07D207/24—Oxygen or sulfur atoms
- C07D207/26—2-Pyrrolidones
- C07D207/263—2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms
- C07D207/267—2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to the ring nitrogen atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
- C07D207/34—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two 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
- C07D207/36—Oxygen or sulfur atoms
-
- 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
- C07D403/06—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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C227/00—Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton
- C07C227/22—Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton from lactams, cyclic ketones or cyclic oximes, e.g. by reactions involving Beckmann rearrangement
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C269/00—Preparation of derivatives of carbamic acid, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
- C07C269/06—Preparation of derivatives of carbamic acid, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups by reactions not involving the formation of carbamate groups
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
- C07C271/06—Esters of carbamic acids
- C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
- C07C271/10—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
- C07C271/22—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by carboxyl groups
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- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
- Y02P20/00—Technologies relating to chemical industry
- Y02P20/50—Improvements relating to the production of bulk chemicals
- Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Hospice & Palliative Care (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Urology & Nephrology (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Pyrrole Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
Abstract
La presente se refiere a procesos para producir inhibidores de NEP o pro-fármacos de los mismos, en particular inhibidores de NEP que comprenden una estructura base de ácido gama-amino-delta-bifenil-alfa-metilalcanoico, o de un éster de ácido. Con detalle, los procesos, de acuerdo con la presente, se relacionan por ultimo con la síntesis de intermediarios para preparar los inhibidores de NEP anteriores, es decir, los compuestos de acuerdo con la formula (1), o una sal de los mismos. Reivindicacion 1: Un proceso para la preparacion de un compuesto de la formula (1), o una sal del mismo: (1) en donde R1 es hidrogeno o un grupo protector de nitrogeno, y R6 y R7 son independientemente un grupo alquilo, un grupo arilo, un grupo aril-alquilo, un grupo cicloalquilo, o juntos R6 y R7 forman un ciclo, junto con el átomo de nitrogeno con el que están unidos, cuyo ciclo puede estar saturado o insaturado, y puede contener opcionalmente uno o más heteroátomos, tales como nitrogeno, oxigeno o azufre, en donde el ciclo contiene de 3 a 8, tal como de 4 a 7 átomos del anillo, comprendiendo este proceso hacer reaccionar un compuesto de la formula (2), o una sal del mismo: (2) en donde R1 es hidrogeno o un grupo protector de nitrogeno, - con una amina de la formula (3), (4), o (5); y opcionalmente una sal, tal como una sal de metal alcalino, una sal de metal alcalinotérreo, una sal amonio, o un líquido ionico; - o con un compuesto preparado mediante la mezcla de un compuesto de la formula (6); con un alcoholato de la formula M-O-R8, y opcionalmente tratar el compuesto mencionado con una sal M1X'; - o con mezclas de los mismos; en donde: cada R6 y cada R7 son independientemente un grupo alquilo, un grupo arilo, un grupo aril-alquilo, un grupo cicloalquilo, o juntos R6 y R7 forman un ciclo, junto con el átomo de nitrogeno con el que están unidos, cuyo ciclo puede estar saturado o insaturado, y puede contener opcionalmente uno o más heteroátomos, tales como nitrogeno, oxígeno, o azufre, en donde el ciclo contiene de 3 a 8, tal como de 4 a 7 átomos del anillo, y cada R8 es independientemente un grupo alquilo, un grupo arilo o un grupo aril-alquilo; X y X' son independientemente un anion, por ejemplo, un haluro, un anion de un ácido sulfonico, un anion de un alquil-sulfato, un tetra-halo-metalato, tal como un tetracloro-metalato, hexafluoro-fosfato, hexafluoro-antimonato, tetrafluoro-borato, perclorato, alcoxido R8-O; en donde R8 se define como antes, carboxilato, o tribromuro; M es un metal alcalino o un metal alcalinotérreo; y M1 es un metal alcalino, un metal alcalinotérreo, o amonio; para obtener el compuesto de la formula (1).
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP08150353 | 2008-01-17 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR070176A1 true AR070176A1 (es) | 2010-03-17 |
Family
ID=40758693
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP090100121A AR070176A1 (es) | 2008-01-17 | 2009-01-15 | Procesos de sintesis de inhibidores de nep, compuestos intermediarios y uso de los mismos en la sintesis |
Country Status (29)
| Country | Link |
|---|---|
| US (4) | US8580974B2 (es) |
| EP (1) | EP2245009B1 (es) |
| JP (2) | JP5739667B2 (es) |
| KR (1) | KR101587668B1 (es) |
| CN (2) | CN103483236B (es) |
| AR (1) | AR070176A1 (es) |
| AU (1) | AU2009204759B2 (es) |
| BR (1) | BRPI0906764A2 (es) |
| CA (1) | CA2711529C (es) |
| CL (1) | CL2009000089A1 (es) |
| CO (1) | CO6290677A2 (es) |
| EC (1) | ECSP10010405A (es) |
| ES (1) | ES2602564T3 (es) |
| GT (1) | GT201000211A (es) |
| HU (1) | HUE030606T2 (es) |
| IL (1) | IL206664A0 (es) |
| MA (1) | MA31951B1 (es) |
| MX (1) | MX2010007842A (es) |
| MY (1) | MY169425A (es) |
| NZ (2) | NZ586657A (es) |
| PE (1) | PE20091364A1 (es) |
| PL (1) | PL2245009T3 (es) |
| PT (1) | PT2245009T (es) |
| RU (2) | RU2513521C2 (es) |
| SG (1) | SG187491A1 (es) |
| SI (1) | SI2245009T1 (es) |
| TN (1) | TN2010000304A1 (es) |
| TW (1) | TWI422370B (es) |
| WO (1) | WO2009090251A2 (es) |
Families Citing this family (52)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR070176A1 (es) * | 2008-01-17 | 2010-03-17 | Novartis Ag | Procesos de sintesis de inhibidores de nep, compuestos intermediarios y uso de los mismos en la sintesis |
| US8450496B2 (en) * | 2009-03-24 | 2013-05-28 | Hoffman-La Roche Inc. | Process for the preparation of propionic acid derivatives |
| ES2602902T3 (es) | 2009-05-28 | 2017-02-22 | Novartis Ag | Derivados aminopropiónicos sustituidos como inhibidores de neprilisina |
| CN102448928B (zh) | 2009-05-28 | 2014-10-01 | 诺华股份有限公司 | 作为中性溶酶(neprilysin)抑制剂的取代的氨基丁酸衍生物 |
| BR112012006406A2 (pt) | 2009-09-23 | 2016-04-12 | Novartis Ag | "processo para a fabrição de n-acilbifenil alanina" |
| JO2967B1 (en) | 2009-11-20 | 2016-03-15 | نوفارتس ايه جي | Acetic acid derivatives of carbamoyl methyl amino are substituted as new NEP inhibitors |
| WO2011088797A1 (en) | 2010-01-22 | 2011-07-28 | Novartis Ag | Intermediates of neutral endopeptidase inhibitors and preparation method thereof |
| KR101476937B1 (ko) * | 2010-08-23 | 2014-12-24 | 노파르티스 아게 | Ｎｅｐ 억제제의 제조를 위한 중간체의 제조 방법 |
| CA2806501A1 (en) * | 2010-08-23 | 2012-03-01 | Novartis Ag | New process for the preparation of intermediates useful for the manufacture nep inhibitors |
| CN103080077B (zh) * | 2010-08-23 | 2015-06-10 | 诺华股份有限公司 | 用于制造nep抑制剂的中间体的制备工艺 |
| US8673974B2 (en) | 2010-11-16 | 2014-03-18 | Novartis Ag | Substituted amino bisphenyl pentanoic acid derivatives as NEP inhibitors |
| CA2819153A1 (en) | 2010-12-15 | 2012-06-21 | Theravance, Inc. | Neprilysin inhibitors |
| HRP20151115T1 (en) | 2010-12-15 | 2015-11-20 | Theravance Biopharma R&D Ip, Llc | Neprilysin inhibitors |
| US8449890B2 (en) | 2011-02-17 | 2013-05-28 | Theravance, Inc. | Neprilysin inhibitors |
| KR101854874B1 (ko) | 2011-02-17 | 2018-05-04 | 세라밴스 바이오파마 알앤디 아이피, 엘엘씨 | 네프릴리신 억제제로서 치환된 아미노부티릭 유도체 |
| CN103596928B (zh) | 2011-05-31 | 2017-02-15 | 施万生物制药研发Ip有限责任公司 | 脑啡肽酶抑制剂 |
| EP2714660B1 (en) | 2011-05-31 | 2018-09-26 | Theravance Biopharma R&D IP, LLC | Neprilysin inhibitors |
| WO2012166389A1 (en) | 2011-05-31 | 2012-12-06 | Theravance, Inc. | Neprilysin inhibitors |
| TWI560172B (en) | 2011-11-02 | 2016-12-01 | Theravance Biopharma R&D Ip Llc | Neprilysin inhibitors |
| ES2609810T3 (es) | 2012-05-31 | 2017-04-24 | Theravance Biopharma R&D Ip, Llc | Inhibidores de neprilisina donadores de óxido nítrico |
| CN104470521B (zh) | 2012-06-08 | 2017-04-12 | 施万生物制药研发Ip有限责任公司 | 脑啡肽酶抑制剂 |
| PT2864292T (pt) | 2012-06-08 | 2017-07-10 | Theravance Biopharma R&D Ip Llc | Inibidores de neprisilina |
| KR102104954B1 (ko) | 2012-08-08 | 2020-04-27 | 세라밴스 바이오파마 알앤디 아이피, 엘엘씨 | 네프릴리신 억제제 |
| TR201808541T4 (tr) | 2013-02-14 | 2018-07-23 | Novartis Ag | Nep (nötr endopeptidaz) inhibitörleri olarak ikame edilmiş bisfenil butanoik fosfonik asit türevleri. |
| EP2956445A1 (en) | 2013-02-14 | 2015-12-23 | Novartis AG | Substituted bisphenyl butanoic acid derivatives as nep inhibitors with improved in vivo efficacy |
| WO2014138053A1 (en) | 2013-03-05 | 2014-09-12 | Theravance Biopharma R&D Ip, Llc | Neprilysin inhibitors |
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| WO2017097275A1 (en) | 2015-12-11 | 2017-06-15 | Zentiva, K.S. | Solid forms of (2r,4s)-5-(biphenyl-4-yl)-4-[(3-carboxypropionyl)amino]-2- -methylpentanoic acid ethyl ester, its salts and a preparation method |
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| WO2011088797A1 (en) * | 2010-01-22 | 2011-07-28 | Novartis Ag | Intermediates of neutral endopeptidase inhibitors and preparation method thereof |
| CA2806501A1 (en) * | 2010-08-23 | 2012-03-01 | Novartis Ag | New process for the preparation of intermediates useful for the manufacture nep inhibitors |
| KR101476937B1 (ko) * | 2010-08-23 | 2014-12-24 | 노파르티스 아게 | Ｎｅｐ 억제제의 제조를 위한 중간체의 제조 방법 |
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