BR112014010576A8 - compostos inibidores de neprilisina (nep), seus usos, processo de preparação dos compostos e composição farmacêutica compreendendo os compostos - Google Patents

compostos inibidores de neprilisina (nep), seus usos, processo de preparação dos compostos e composição farmacêutica compreendendo os compostos Download PDF

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Publication number
BR112014010576A8
BR112014010576A8 BR112014010576A BR112014010576A BR112014010576A8 BR 112014010576 A8 BR112014010576 A8 BR 112014010576A8 BR 112014010576 A BR112014010576 A BR 112014010576A BR 112014010576 A BR112014010576 A BR 112014010576A BR 112014010576 A8 BR112014010576 A8 BR 112014010576A8
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compounds
neprilisin
nep
preparing
pharmaceutical composition
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BR112014010576A
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BR112014010576B8 (pt
BR112014010576B1 (pt
BR112014010576A2 (pt
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Hughes Adam
J Moran Edmund
Fenster Erik
Fleury Melissa
Gendron Roland
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Theravance Biopharma R&D Ip Llc
Theravance Inc
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Publication of BR112014010576A2 publication Critical patent/BR112014010576A2/pt
Publication of BR112014010576A8 publication Critical patent/BR112014010576A8/pt
Publication of BR112014010576B1 publication Critical patent/BR112014010576B1/pt
Publication of BR112014010576B8 publication Critical patent/BR112014010576B8/pt

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19Carboxylic acids, e.g. valproic acid
    • A61K31/195Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/197Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/21Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/216Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acids having aromatic rings, e.g. benactizyne, clofibrate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/21Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/235Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group
    • A61K31/24Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group having an amino or nitro group
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/21Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/27Esters, e.g. nitroglycerine, selenocyanates of carbamic or thiocarbamic acids, meprobamate, carbachol, neostigmine
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    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/365Lactones
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
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    • AHUMAN NECESSITIES
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    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
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    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C231/00Preparation of carboxylic acid amides
    • C07C231/02Preparation of carboxylic acid amides from carboxylic acids or from esters, anhydrides, or halides thereof by reaction with ammonia or amines
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    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00Carboxylic acid amides
    • C07C233/01Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/56Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having carbon atoms of carboxamide groups bound to carbon atoms of carboxyl groups, e.g. oxamides
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C241/00Preparation of compounds containing chains of nitrogen atoms singly-bound to each other, e.g. hydrazines, triazanes
    • C07C241/04Preparation of hydrazides
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    • C07C243/00Compounds containing chains of nitrogen atoms singly-bound to each other, e.g. hydrazines, triazanes
    • C07C243/24Hydrazines having nitrogen atoms of hydrazine groups acylated by carboxylic acids
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    • C07C243/24Hydrazines having nitrogen atoms of hydrazine groups acylated by carboxylic acids
    • C07C243/26Hydrazines having nitrogen atoms of hydrazine groups acylated by carboxylic acids with acylating carboxyl groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C243/28Hydrazines having nitrogen atoms of hydrazine groups acylated by carboxylic acids with acylating carboxyl groups bound to hydrogen atoms or to acyclic carbon atoms to hydrogen atoms or to carbon atoms of a saturated carbon skeleton
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    • C07C243/24Hydrazines having nitrogen atoms of hydrazine groups acylated by carboxylic acids
    • C07C243/26Hydrazines having nitrogen atoms of hydrazine groups acylated by carboxylic acids with acylating carboxyl groups bound to hydrogen atoms or to acyclic carbon atoms
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    • C07C271/06Esters of carbamic acids
    • C07C271/08Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/10Esters 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
    • C07C271/22Esters 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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    • C07D207/18Heterocyclic 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
    • C07D207/22Heterocyclic 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
    • C07D207/24Oxygen or sulfur atoms
    • C07D207/262-Pyrrolidones
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    • C07D317/08Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3
    • C07D317/10Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 not condensed with other rings
    • C07D317/32Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 not condensed with other rings 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
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    • C07D319/061,3-Dioxanes; Hydrogenated 1,3-dioxanes not condensed with other rings
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    • A61K31/165Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A61K31/166Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the carbon of a carboxamide group directly attached to the aromatic ring, e.g. procainamide, procarbazine, metoclopramide, labetalol
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
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    • A61K31/165Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A61K31/167Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol

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  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Pulmonology (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Abstract

resumo inibidores de neprilisina em um aspecto, a invenção refere-se a compostos tendo a fórmula: (i) em que r1-r6, a, b, e z são como definidos na especificação, ou um seu sal farmaceuticamente aceitável. estes compostos têm atividade de inibição de neprilisina. em outro aspecto, a invenção refere-se a composições farmacêuticas compreendendo esses compostos; métodos de utilização de tais compostos; e processos e intermediários para a preparação de tais compostos.
BR112014010576A 2011-11-02 2012-11-01 compostos inibidores de neprilisina (nep), seus usos, processo de preparação dos compostos e composição farmacêutica compreendendo os compostos BR112014010576B8 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161554625P 2011-11-02 2011-11-02
US61/554,625 2011-11-02
PCT/US2012/063036 WO2013067163A1 (en) 2011-11-02 2012-11-01 Neprilysin inhibitors

Publications (4)

Publication Number Publication Date
BR112014010576A2 BR112014010576A2 (pt) 2017-05-02
BR112014010576A8 true BR112014010576A8 (pt) 2020-05-19
BR112014010576B1 BR112014010576B1 (pt) 2020-05-26
BR112014010576B8 BR112014010576B8 (pt) 2020-12-08

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BR112014010576A BR112014010576B8 (pt) 2011-11-02 2012-11-01 compostos inibidores de neprilisina (nep), seus usos, processo de preparação dos compostos e composição farmacêutica compreendendo os compostos

Country Status (30)

Country Link
US (7) US8691868B2 (pt)
EP (1) EP2773335B1 (pt)
JP (1) JP5944010B2 (pt)
KR (1) KR102013200B1 (pt)
CN (1) CN103906509B (pt)
AR (1) AR088618A1 (pt)
AU (1) AU2012332422B2 (pt)
BR (1) BR112014010576B8 (pt)
CA (1) CA2850953C (pt)
CO (1) CO6940421A2 (pt)
CY (1) CY1118909T1 (pt)
DK (1) DK2773335T3 (pt)
ES (1) ES2625628T3 (pt)
HK (1) HK1200371A1 (pt)
HR (1) HRP20170646T1 (pt)
HU (1) HUE034647T2 (pt)
IL (1) IL232038A (pt)
LT (1) LT2773335T (pt)
ME (1) ME02726B (pt)
MX (1) MX343753B (pt)
MY (1) MY165087A (pt)
PL (1) PL2773335T3 (pt)
PT (1) PT2773335T (pt)
RS (1) RS55947B1 (pt)
RU (1) RU2629930C2 (pt)
SG (2) SG10201509182YA (pt)
SI (1) SI2773335T1 (pt)
TW (1) TWI560172B (pt)
WO (1) WO2013067163A1 (pt)
ZA (1) ZA201402636B (pt)

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CA2817368C (en) 2010-12-15 2019-12-31 Theravance, Inc. Neprilysin inhibitors
AR084290A1 (es) 2010-12-15 2013-05-08 Theravance Inc Inhibidores de neprilisina, metodos para su preparacion e intermediarios utilizados en los mismos, composiciones farmaceuticas que los comprenden y su uso en la fabricacion de medicamentos para tratar enfermedades mediadas por la inhibicion de nep
US8449890B2 (en) 2011-02-17 2013-05-28 Theravance, Inc. Neprilysin inhibitors
ES2582640T3 (es) 2011-02-17 2016-09-14 Theravance Biopharma R&D Ip, Llc Derivados aminobutíricos sustituidos como inhibidores de neprilisina
CA2835216A1 (en) 2011-05-31 2012-12-06 Theravance, Inc. Neprilysin inhibitors
CN202237001U (zh) * 2011-07-01 2012-05-30 龙泰兴业有限公司 具防护围网的跳床结构
TWI560172B (en) 2011-11-02 2016-12-01 Theravance Biopharma R&D Ip Llc Neprilysin inhibitors
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PT2864292T (pt) 2012-06-08 2017-07-10 Theravance Biopharma R&D Ip Llc Inibidores de neprisilina
US8871792B2 (en) 2012-06-08 2014-10-28 Theravance Biopharma R&D Ip, Llc Neprilysin inhibitors
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CA2902456A1 (en) 2013-03-05 2014-09-12 Theravance Biopharma R&D Ip, Llc Neprilysin inhibitors
RU2016135057A (ru) * 2014-01-30 2018-03-12 ТЕРЕВАНС БАЙОФАРМА Ар энд Ди АйПи, ЭлЭлСи Производные 5-бифенил-4-гетероарилкарбониламинопентановой кислоты в качестве ингибиторов неприлизина
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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
WO2016029828A1 (zh) * 2014-08-27 2016-03-03 上海翰森生物医药科技有限公司 AHU-377结晶型游离酸、半钙盐、α﹣苯乙胺盐及其制备方法和应用
CN107074744B (zh) * 2014-12-03 2019-06-18 上海翰森生物医药科技有限公司 Nep抑制剂结晶型游离酸、钙盐多晶型及其制备方法和应用
MY187899A (en) 2015-02-11 2021-10-27 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
HUE052732T2 (hu) 2015-02-19 2021-05-28 Theravance Biopharma R&D Ip Llc (2R,4R)-5-(5'-klór-2'-fluorbifenil-4-il)-2-hidroxi-4-[(5-metiloxazol-2-karbonil)amino]pentánsav
CN105330569A (zh) * 2015-09-11 2016-02-17 天台宜生生化科技有限公司 一种(r)-2-(n-叔丁氧羰基氨基)联苯丙醇的制备方法
CN106310270A (zh) * 2015-12-18 2017-01-11 深圳奥萨制药有限公司 血管紧张素转化酶抑制剂与脑啡肽酶抑制剂的药物组合物
CN106310271A (zh) * 2016-01-27 2017-01-11 深圳奥萨制药有限公司 一种治疗慢性心力衰竭的药物组合物
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