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MX2012008483A - Intermediarios de inhibidores de la endopeptidasa neutra y metodo de preparacion de los mismos. - Google Patents

Intermediarios de inhibidores de la endopeptidasa neutra y metodo de preparacion de los mismos.

Info

Publication number
MX2012008483A
MX2012008483A MX2012008483A MX2012008483A MX2012008483A MX 2012008483 A MX2012008483 A MX 2012008483A MX 2012008483 A MX2012008483 A MX 2012008483A MX 2012008483 A MX2012008483 A MX 2012008483A MX 2012008483 A MX2012008483 A MX 2012008483A
Authority
MX
Mexico
Prior art keywords
intermediates
preparation
neutral endopeptidase
endopeptidase inhibitors
inhibitors
Prior art date
Application number
MX2012008483A
Other languages
English (en)
Inventor
David Hook
Jianguang Zhou
Yunzhong Li
Jie Ku
Original Assignee
Novartis Ag
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of MX2012008483A publication Critical patent/MX2012008483A/es

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    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C231/00—Preparation of carboxylic acid amides
    • C07C231/10—Preparation of carboxylic acid amides from compounds not provided for in groups C07C231/02 - C07C231/08
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/4015—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil having oxo groups directly attached to the heterocyclic ring, e.g. piracetam, ethosuximide
    • 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
    • C07D207/18—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
    • C07D207/27—2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms with substituted hydrocarbon radicals 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
    • C07D207/18—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
    • C07D207/273—2-Pyrrolidones 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 other ring carbon atoms
    • C07D207/277—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Hematology (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Diabetes (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pyrrole Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Se dan a conocer intermediarios para la elaboración de inhibidores de la endopeptídasa neutra (NEP) o de pro-fármacos de los mismos, y un método para la preparación de los mismos. En particular, los inhibidores de la endopeptidasa neutra (NEP) comprenden una estructura base de ácido y-amino-d-bifenil-a-metil- alcanoico o de éster de ácido, tal como de etil-éster del ácido N-(3- carboxil-1 -oxo-propil)-(4S)-(p-fenil-fenil-metil)-4-amino-( 2R)-metil-butanoico o de una sal del mismo.
MX2012008483A 2010-01-22 2011-01-21 Intermediarios de inhibidores de la endopeptidasa neutra y metodo de preparacion de los mismos. MX2012008483A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN2010070322 2010-01-22
PCT/CN2011/070458 WO2011088797A1 (en) 2010-01-22 2011-01-21 Intermediates of neutral endopeptidase inhibitors and preparation method thereof

Publications (1)

Publication Number Publication Date
MX2012008483A true MX2012008483A (es) 2012-08-15

Family

ID=44306404

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2012008483A MX2012008483A (es) 2010-01-22 2011-01-21 Intermediarios de inhibidores de la endopeptidasa neutra y metodo de preparacion de los mismos.

Country Status (16)

Country Link
US (2) US9067883B2 (es)
EP (1) EP2526088B1 (es)
JP (1) JP5600183B2 (es)
KR (1) KR101463670B1 (es)
CN (2) CN102712585B (es)
AU (1) AU2011207020B2 (es)
BR (1) BR112012017869A2 (es)
CA (1) CA2786929C (es)
ES (1) ES2550485T3 (es)
HR (1) HRP20151061T1 (es)
MX (1) MX2012008483A (es)
PL (1) PL2526088T3 (es)
PT (1) PT2526088E (es)
RU (1) RU2564024C2 (es)
SI (1) SI2526088T1 (es)
WO (1) WO2011088797A1 (es)

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PE20091364A1 (es) * 2008-01-17 2009-10-13 Novartis Ag Proceso para la preparacion de inhibidores de nep
MX2012008483A (es) * 2010-01-22 2012-08-15 Novartis Ag Intermediarios de inhibidores de la endopeptidasa neutra y metodo de preparacion de los mismos.
SI2609075T1 (sl) 2010-08-23 2016-06-30 Novartis Ag Postopek za pripravo intermediatov za izdelavo NEP inhibitorjev
SG191175A1 (en) 2010-12-15 2013-07-31 Theravance Inc Neprilysin inhibitors
PH12013501240A1 (en) 2010-12-15 2015-09-16 Theravance Biopharma R & D Ip Llc Neprilysin inhibitors
EP2675792B1 (en) 2011-02-17 2016-01-06 Theravance Biopharma R&D IP, LLC Substituted aminobutyric derivatives as neprilysin inhibitors
WO2012112742A1 (en) 2011-02-17 2012-08-23 Theravance, Inc. Substituted aminobutyric derivatives as neprilysin inhibitors
WO2012166390A1 (en) 2011-05-31 2012-12-06 Theravance, Inc. Neprilysin inhibitors
ES2653215T3 (es) 2011-05-31 2018-02-06 Theravance Biopharma R&D Ip, Llc Inhibidores de neprilisina
CN103748070B (zh) 2011-05-31 2015-06-24 施万生物制药研发Ip有限责任公司 脑啡肽酶抑制剂
TWI560172B (en) 2011-11-02 2016-12-01 Theravance Biopharma R&D Ip Llc Neprilysin inhibitors
TWI562986B (en) * 2012-02-15 2016-12-21 Theravance Biopharma R&D Ip Llc Process for preparing 4-amino-5-biphenyl-4-yl-2-hydroxymethyl-2-methyl-pentanoic acid compounds
EP2855464B1 (en) 2012-05-31 2016-10-26 Theravance Biopharma R&D IP, LLC Nitric oxide donor neprilysin inhibitors
KR102102197B1 (ko) 2012-06-08 2020-04-20 세라밴스 바이오파마 알앤디 아이피, 엘엘씨 네프릴리신 억제제
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
NZ704741A (en) 2012-08-08 2017-10-27 Theravance Biopharma R&D Ip Llc Neprilysin inhibitors
CA2902456A1 (en) 2013-03-05 2014-09-12 Theravance Biopharma R&D Ip, Llc Neprilysin inhibitors
EP3099668B1 (en) 2014-01-30 2022-05-04 Theravance Biopharma R&D IP, LLC 5-biphenyl-4-heteroarylcarbonylamino-pentanoic acid derivatives as neprilysin inhibitors
KR20160113291A (ko) 2014-01-30 2016-09-28 세라밴스 바이오파마 알앤디 아이피, 엘엘씨 네프리리신 저해제
CN106795099B (zh) * 2014-04-10 2019-11-26 南京奥昭生物科技有限公司 用于治疗高血压和心血管疾病的前药和组合物
PT3218351T (pt) 2014-11-14 2019-09-26 Zentiva Ks Um método para a preparação, isolamento e purificação de formas farmaceuticamente aplicáveis de ahu-377
SG11201706308RA (en) 2015-02-11 2017-09-28 Theravance Biopharma R&D Ip Llc (2s,4r)-5-(5'-chloro-2'-fluorobiphenyl-4-yl)-4-(ethoxyoxalylamino)-2-hydroxymethyl-2-methylpentanoic acid as neprilysin inhibitor
TW201632493A (zh) 2015-02-13 2016-09-16 諾華公司 新穎方法
CN107250119B (zh) 2015-02-19 2020-09-22 施万生物制药研发Ip有限责任公司 (2r,4r)-5-(5′-氯-2′-氟联苯-4-基)-2-羟基-4-[(5-甲基恶唑-2-羰基)氨基]戊酸
CN104860894B (zh) * 2015-06-10 2017-05-17 北京博全健医药科技有限公司 一种抗心衰药lcz696的制备方法
WO2017051326A1 (en) 2015-09-23 2017-03-30 Novartis Ag New processes and intermediates useful in synthesis of nep inhibitors
CA3006254A1 (en) 2015-12-10 2017-06-15 Novartis Ag New process and intermediates
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
SMT202100434T1 (it) 2016-03-08 2021-09-14 Theravance Biopharma R&D Ip Llc Acido (2s,4r)-5-(5’-cloro-2-fluoro-[1,1’-bifenil]-4-il)-2-(etossimetil)-4-(3-idrossiisossazol-5-carbossammido)-2-metilpentanoico cristallino e suoi usi
CN109415308B (zh) 2016-07-05 2022-09-06 诺华股份有限公司 用于早期沙卡布曲中间体的新方法
US10851059B2 (en) 2016-08-17 2020-12-01 Novartis Ag Processes and intermediates for NEP inhibitor synthesis
CN106380421B (zh) * 2016-08-26 2017-12-08 中国科学院上海有机化学研究所 沙库必曲的合成方法
WO2018116203A1 (en) 2016-12-23 2018-06-28 Novartis Ag New process for early sacubitril intermediates
EP3611160B1 (en) 2017-04-28 2023-03-29 Wuhan LL Science And Technology Development Co., Ltd. Ammonium carboxylate compound, crystal form and amorphous substance thereof, and preparation method therefor
CN112094198B (zh) * 2020-06-15 2025-02-11 南京红太阳医药研究院有限公司 一种n-亚硝基-n-甲基-4-氨基丁酸的合成方法

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JPH11152267A (ja) * 1997-11-20 1999-06-08 Mitsui Chem Inc ピロリジノン誘導体の製造方法
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EP1903027A1 (en) * 2006-09-13 2008-03-26 Novartis AG Process for preparing biaryl substituted 4-amino-butyric acid or derivatives thereof and their use in the production of NEP inhibitors
NZ577910A (en) * 2007-01-12 2012-04-27 Novartis Ag Process for preparing 5-biphenyl-4-amino-2-methyl pentanoic acid
PE20091364A1 (es) * 2008-01-17 2009-10-13 Novartis Ag Proceso para la preparacion de inhibidores de nep
MX2012008483A (es) * 2010-01-22 2012-08-15 Novartis Ag Intermediarios de inhibidores de la endopeptidasa neutra y metodo de preparacion de los mismos.

Also Published As

Publication number Publication date
HRP20151061T1 (hr) 2015-12-04
AU2011207020B2 (en) 2014-04-17
EP2526088A1 (en) 2012-11-28
SI2526088T1 (sl) 2015-12-31
EP2526088B1 (en) 2015-08-05
CN102712585B (zh) 2015-06-24
WO2011088797A1 (en) 2011-07-28
ES2550485T3 (es) 2015-11-10
RU2564024C2 (ru) 2015-09-27
KR101463670B1 (ko) 2014-11-19
US20150274642A1 (en) 2015-10-01
JP2013517306A (ja) 2013-05-16
CN102712585A (zh) 2012-10-03
RU2012135772A (ru) 2014-02-27
US9067883B2 (en) 2015-06-30
CA2786929C (en) 2017-10-24
AU2011207020A1 (en) 2012-08-09
PT2526088E (pt) 2015-11-03
US9278908B2 (en) 2016-03-08
CN104262228B (zh) 2017-01-18
CN104262228A (zh) 2015-01-07
US20120289710A1 (en) 2012-11-15
KR20120120947A (ko) 2012-11-02
CA2786929A1 (en) 2011-07-28
JP5600183B2 (ja) 2014-10-01
EP2526088A4 (en) 2013-08-21
BR112012017869A2 (pt) 2019-09-24
PL2526088T3 (pl) 2016-01-29

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