AR083873A1 - Derivados de acido amino-fenil-pentanoico sustituidos como inhibidores de nep - Google Patents

Derivados de acido amino-fenil-pentanoico sustituidos como inhibidores de nep

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Publication number
AR083873A1
AR083873A1 ARP110104250A ARP110104250A AR083873A1 AR 083873 A1 AR083873 A1 AR 083873A1 AR P110104250 A ARP110104250 A AR P110104250A AR P110104250 A ARP110104250 A AR P110104250A AR 083873 A1 AR083873 A1 AR 083873A1
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AR
Argentina
Prior art keywords
alkyl
phenyl
amino
acid derivatives
pentanoic acid
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Application number
ARP110104250A
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English (en)
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.)
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Publication date
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of AR083873A1 publication Critical patent/AR083873A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/70—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton
    • C07C235/72—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton with the carbon atoms of the carboxamide groups bound to acyclic carbon atoms
    • C07C235/74—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton with the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of a saturated carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/70—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton
    • 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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/192—Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid 
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    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/216—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acids having aromatic rings, e.g. benactizyne, clofibrate
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  • Diabetes (AREA)
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  • Heart & Thoracic Surgery (AREA)
  • Obesity (AREA)
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  • Urology & Nephrology (AREA)
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  • Pulmonology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Epidemiology (AREA)
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  • Child & Adolescent Psychology (AREA)
  • Rheumatology (AREA)
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Abstract

Reivindicación 1: Un compuesto de la fórmula (1), en donde: X y X1 son independientemente OH, -O-alquilo C1-7, NRaRb, -NHS(O)2-alquilo C1-7 o -NHS(O)2-bencilo, en donde Ra y Rb, por cada presentación, son independientemente H o alquilo C1-7; R1 es H o alquilo C1-6; R2 por cada presentación, es independientemente alcoxilo C1-6, hidroxilo, halógeno, alquilo C1-6, ciano o halo-alquilo C1-6; A1 es un alquileno C1-4 lineal; R3 por cada presentación, es independientemente halógeno, hidroxilo, alcoxilo C1-7, halógeno, alquilo C1-7, o halo-alquilo C1-7; o n es un entero de 1 a 5; s es 0 o un entero de 1 a 4; o una sal farmacéuticamente aceptable del mismo.
ARP110104250A 2010-11-16 2011-11-14 Derivados de acido amino-fenil-pentanoico sustituidos como inhibidores de nep AR083873A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US41416310P 2010-11-16 2010-11-16

Publications (1)

Publication Number Publication Date
AR083873A1 true AR083873A1 (es) 2013-03-27

Family

ID=45093705

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP110104250A AR083873A1 (es) 2010-11-16 2011-11-14 Derivados de acido amino-fenil-pentanoico sustituidos como inhibidores de nep

Country Status (14)

Country Link
US (1) US8673974B2 (es)
EP (1) EP2640690A1 (es)
JP (1) JP5872575B2 (es)
KR (1) KR101951492B1 (es)
CN (1) CN103201257B (es)
AR (1) AR083873A1 (es)
AU (1) AU2011331294B2 (es)
BR (1) BR112013011580A2 (es)
CA (1) CA2817114A1 (es)
EA (1) EA021537B1 (es)
MX (1) MX2013005533A (es)
TW (1) TW201305089A (es)
UY (1) UY33731A (es)
WO (1) WO2012065956A1 (es)

Families Citing this family (26)

* Cited by examiner, † Cited by third party
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PT2183273T (pt) 2007-08-17 2017-05-22 Novartis Ag Depsipéptidos cíclicos
HUE028051T2 (hu) 2010-12-15 2016-11-28 Theravance Biopharma R&D Ip Llc Neprilizin inhibitorok
CA2819153A1 (en) 2010-12-15 2012-06-21 Theravance, Inc. Neprilysin inhibitors
JP5959065B2 (ja) 2011-02-17 2016-08-02 セラヴァンス バイオファーマ アール＆ディー アイピー， エルエルシー ネプリライシン阻害剤としての置換アミノ酪酸誘導体
JP5959066B2 (ja) 2011-02-17 2016-08-02 セラヴァンス バイオファーマ アール＆ディー アイピー， エルエルシー ネプリライシン阻害剤としての置換アミノ酪酸誘導体
CN103582630B (zh) 2011-05-31 2016-08-17 施万生物制药研发Ip有限责任公司 脑啡肽酶抑制剂
JP5959074B2 (ja) 2011-05-31 2016-08-02 セラヴァンス バイオファーマ アール＆ディー アイピー， エルエルシー ネプリライシン阻害剤
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
CA2871292A1 (en) 2012-05-31 2013-12-05 Theravance Biopharma R&D Ip, Llc Nitric oxide donor neprilysin inhibitors
WO2013184898A1 (en) 2012-06-08 2013-12-12 Theravance, Inc. Neprilysin inhibitors
SMT201700306T1 (it) 2012-06-08 2017-07-18 Theravance Biopharma R&D Ip Llc Inibitori di neprilisina
MX366149B (es) 2012-08-08 2019-06-28 Theravance Biopharma R&D Ip Llc Inhibidores de neprilisina.
DK2964616T3 (en) 2013-03-05 2017-08-28 Theravance Biopharma R&D Ip Llc Neprilysin inhibitors
CA2934898A1 (en) 2014-01-30 2015-08-06 Theravance Biopharma R&D Ip, Llc 5-biphenyl-4-heteroarylcarbonylamino-pentanoic acid derivatives as neprilysin inhibitors
CA2934936A1 (en) 2014-01-30 2015-08-06 Theravance Biopharma R&D Ip, Llc Neprilysin inhibitors
BR112017013465A2 (pt) * 2014-12-24 2018-03-06 Lg Chem, Ltd derivado de biarila, e, composição farmacêutica.
CN104557600B (zh) * 2015-01-26 2016-05-04 苏州明锐医药科技有限公司 沙库比曲的制备方法
JP6766055B2 (ja) 2015-02-11 2020-10-07 セラヴァンス バイオファーマ アール＆ディー アイピー， エルエルシー ネプリライシン阻害剤としての（２ｓ，４ｒ）−５−（５’−クロロ−２’−フルオロビフェニル−４−イル）−４−（エトキシオキサリルアミノ）−２−ヒドロキシメチル−２−メチルペンタン酸
LT3259255T (lt) 2015-02-19 2021-04-26 Theravance Biopharma R&D Ip, Llc (2r,4r)-5-(5`-chlor-2`-fluorbifenil-4-il)-2-hidroksi-4-[(5-metiloksazol-2-karbonil)amino]pentano rūgštis
JP7306828B2 (ja) 2016-03-08 2023-07-11 セラヴァンス バイオファーマ アール＆ディー アイピー， エルエルシー 結晶性（２ｓ，４ｒ）－５－（５’－クロロ－２’－フルオロ－［１，１’－ビフェニル］－４－イル）－２－（エトキシメチル）－４－（３－ヒドロキシイソオキサゾール－５－カルボキサミド）－２－メチルペンタン酸およびその使用
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
JP2022507958A (ja) 2018-11-27 2022-01-18 ノバルティス アーゲー 代謝障害の治療用のプロタンパク質転換酵素サブチリシン／ケキシン９型（ｐｃｓｋ９）阻害薬としての環状四量体化合物
PY1998404A (es) 2018-11-27 2021-06-17 Novartis Ag Compuestos tetrámeros cíclicos como inhibidores de proproteína convertasa subtilisina/kexina tipo 9 (pcsk9) para el tratamiento de trastornos metabólicos
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CA2817114A1 (en) 2012-05-24
EA201390723A1 (ru) 2013-09-30
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AU2011331294A1 (en) 2013-05-02
BR112013011580A2 (pt) 2016-08-09
KR101951492B1 (ko) 2019-02-22
US20120122977A1 (en) 2012-05-17
JP5872575B2 (ja) 2016-03-01
WO2012065956A1 (en) 2012-05-24
MX2013005533A (es) 2013-07-03
EA021537B1 (ru) 2015-07-30
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