MX2018010727A - Acido (2s,4r)-5-(5'-cloro-2'-fluoro-[1,1'-bifenil]-4-il)-2-(etoxim etil)-4-(3-hidroxiisoxazol-5-carboxamido)-2-metilpentanoico cristalino, y sus usos. - Google Patents

Acido (2s,4r)-5-(5'-cloro-2'-fluoro-[1,1'-bifenil]-4-il)-2-(etoxim etil)-4-(3-hidroxiisoxazol-5-carboxamido)-2-metilpentanoico cristalino, y sus usos.

Info

Publication number
MX2018010727A
MX2018010727A MX2018010727A MX2018010727A MX2018010727A MX 2018010727 A MX2018010727 A MX 2018010727A MX 2018010727 A MX2018010727 A MX 2018010727A MX 2018010727 A MX2018010727 A MX 2018010727A MX 2018010727 A MX2018010727 A MX 2018010727A
Authority
MX
Mexico
Prior art keywords
crystalline
hydroxyisoxazole
carboxamido
ethoxymethyl
biphenyl
Prior art date
Application number
MX2018010727A
Other languages
English (en)
Inventor
Fleury Melissa
Rapta Miroslav
d hughes Adam
Timothy Fass Gene
R Thalladi Venkat
Simeone Michael
Michael Baldwin R
L Bourdet David
Original Assignee
Theravance Biopharma R&D Ip Llc
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 Theravance Biopharma R&D Ip Llc filed Critical Theravance Biopharma R&D Ip Llc
Publication of MX2018010727A publication Critical patent/MX2018010727A/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
    • C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
    • C07D261/06—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
    • C07D261/10—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more 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
    • C07D261/18—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4816—Wall or shell material
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

Abstract

En un aspecto, la invención se refiere a una forma cristalina de la estructura: (ver Fórmula) o una sal farmacéuticamente aceptable de la misma, que tiene actividad inhibitoria de la neprilisina. En otro aspecto, la invención se refiere a composiciones farmacéuticas que comprenden esta forma cristalina; métodos de uso de esta forma cristalina y su forma soluble (I); y procesos para preparar formas solubles (I) y cristalinas (I´).
MX2018010727A 2016-03-08 2017-03-07 Acido (2s,4r)-5-(5'-cloro-2'-fluoro-[1,1'-bifenil]-4-il)-2-(etoxim etil)-4-(3-hidroxiisoxazol-5-carboxamido)-2-metilpentanoico cristalino, y sus usos. MX2018010727A (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662305393P 2016-03-08 2016-03-08
US201662346336P 2016-06-06 2016-06-06
PCT/US2017/021172 WO2017156009A1 (en) 2016-03-08 2017-03-07 Crystalline(2s,4r)-5-(5'-chloro-2'-fluoro-[1,1'-biphenyl]-4-yl)-2-(ethoxymethyl)-4-(3-hydroxyisoxazole-5-carboxamido)-2-methylpentanoic acid and uses thereof

Publications (1)

Publication Number Publication Date
MX2018010727A true MX2018010727A (es) 2019-01-24

Family

ID=58387911

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2018010727A MX2018010727A (es) 2016-03-08 2017-03-07 Acido (2s,4r)-5-(5'-cloro-2'-fluoro-[1,1'-bifenil]-4-il)-2-(etoxim etil)-4-(3-hidroxiisoxazol-5-carboxamido)-2-metilpentanoico cristalino, y sus usos.

Country Status (29)

Country Link
US (5) US10100021B2 (es)
EP (1) EP3408260B1 (es)
JP (2) JP7306828B2 (es)
KR (2) KR20180114225A (es)
CN (1) CN108779084A (es)
AU (1) AU2017229466C1 (es)
BR (1) BR112018068170A2 (es)
CA (1) CA3015505C (es)
CL (1) CL2018002539A1 (es)
CO (1) CO2018010568A2 (es)
CY (1) CY1124397T1 (es)
DK (1) DK3408260T3 (es)
ES (1) ES2880123T3 (es)
HR (1) HRP20211169T1 (es)
HU (1) HUE055546T2 (es)
IL (1) IL261244B (es)
LT (1) LT3408260T (es)
MX (1) MX2018010727A (es)
PH (1) PH12018501876A1 (es)
PL (1) PL3408260T3 (es)
PT (1) PT3408260T (es)
RS (1) RS62172B1 (es)
RU (1) RU2756223C2 (es)
SA (1) SA518392325B1 (es)
SG (1) SG11201807591VA (es)
SI (1) SI3408260T1 (es)
TW (1) TWI731943B (es)
WO (1) WO2017156009A1 (es)
ZA (1) ZA201805840B (es)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI731943B (zh) 2016-03-08 2021-07-01 美商施萬生物製藥研發Ｉｐ有限責任公司 結晶型（2s，4r）－5－（5’－氯－2’－氟－［1，1’－聯苯］－4－基）－2－（乙氧基甲基）－4－（3－羥基異㗁唑－5－甲醯胺基）－2－甲基戊酸及其用途
CA3151788A1 (en) * 2019-09-20 2021-03-25 Jingchao Sun Uses of complex of angiotensin ii receptor antagonist metabolite and nep inhibitor in treating heart failure
KR102485499B1 (ko) * 2022-07-15 2023-01-09 오가노이드사이언스 주식회사 신장 질환의 치료 또는 예방용 조성물

Family Cites Families (49)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4189604A (en) 1975-07-22 1980-02-19 Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai Bestatin
US4206232A (en) 1976-05-10 1980-06-03 E. R. Squibb & Sons, Inc. Relieving hypertension with carboxyalkylacylamino acids
IL58849A (en) 1978-12-11 1983-03-31 Merck & Co Inc Carboxyalkyl dipeptides and derivatives thereof,their preparation and pharmaceutical compositions containing them
FR2480747A1 (fr) 1980-04-17 1981-10-23 Roques Bernard Derives d'acides amines et leur application therapeutique
US4906615A (en) 1980-12-18 1990-03-06 Schering Corporation Substituted dipeptides as inhibitors of enkephalinases
US4722810A (en) 1984-08-16 1988-02-02 E. R. Squibb & Sons, Inc. Enkephalinase inhibitors
US4939261A (en) 1984-06-08 1990-07-03 Ciba-Geigy Corporation N-substituted butyramide derivatives useful for treatment of conditions responsive to inhibition of enkephalinase
EP0225292A3 (en) 1985-12-06 1988-11-30 Ciba-Geigy Ag Certain n-substituted butyramide derivatives
US4929641B1 (en) 1988-05-11 1994-08-30 Schering Corp Mercapto-acylamino acid antihypertensives
KR880007441A (ko) 1986-12-11 1988-08-27 알렌 제이.스피겔 스피로-치환된 글루타르아미드 이뇨제
FR2623498B1 (fr) 1987-11-24 1990-04-06 Bioprojet Soc Civ Nouveaux composes enantiomeres derives d'amino-acides, leur procede de preparation et leurs applications therapeutiques
GB8820844D0 (en) 1988-09-05 1988-10-05 Pfizer Ltd Therapeutic agents
US5599951A (en) 1989-09-15 1997-02-04 Societe Civile Bioprojet Amino acid derivatives, the process for their preparation and their applications to therapy
US5155100A (en) 1991-05-01 1992-10-13 Ciba-Geigy Corporation Phosphono/biaryl substituted dipeptide derivatives
US5294632A (en) 1991-05-01 1994-03-15 Ciba-Geigy Corporation Phosphono/biaryl substituted dipetide derivatives
US5217996A (en) 1992-01-22 1993-06-08 Ciba-Geigy Corporation Biaryl substituted 4-amino-butyric acid amides
US5508272A (en) 1993-06-15 1996-04-16 Bristol-Myers Squibb Company Compounds containing a fused bicycle ring and processes therefor
DE19510566A1 (de) 1995-03-23 1996-09-26 Kali Chemie Pharma Gmbh Benzazepin-, Benzoxazepin- und Benzothiazepin-N-essigsäurederivate sowie Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende Arzneimittel
EP0821670A1 (en) 1995-04-21 1998-02-04 Novartis AG N-aroylamino acid amides as endothelin inhibitors
US6660756B2 (en) 2001-03-28 2003-12-09 Pfizer Inc. N-phenpropylcyclopentyl-substituted glutaramide derivatives as inhibitors of neutral endopeptidase
GB0119305D0 (en) 2001-04-12 2001-10-03 Aventis Pharma Gmbh Mercaptoacetylamide derivatives,a process for their preparation and their use
WO2006027680A1 (en) 2004-09-10 2006-03-16 Pfizer Limited 3-(1-carbamoylcyclohexyl) propionic acid derivatives as inhibitors of neutral endopeptidase enzyme
AR057882A1 (es) 2005-11-09 2007-12-26 Novartis Ag Compuestos de accion doble de bloqueadores del receptor de angiotensina e inhibidores de endopeptidasa neutra
CA2637588A1 (en) 2006-02-17 2007-08-30 Monsanto Technology Llc Chimeric regulatory sequences comprising introns from dicotyledons for plant gene expression
WO2007106708A2 (en) 2006-03-10 2007-09-20 Novartis Ag Combinations of the angiotensin ii antagonist valsartan and the nep inhibitor daglutril
MX2009007474A (es) 2007-01-12 2009-10-08 Novartis Ag Proceso para la preparacion de acido 5-bifenil-4-amino-2-metil pentanoico.
TWI448284B (zh) 2007-04-24 2014-08-11 Theravance Inc 雙效抗高血壓劑
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
EA201101672A1 (ru) 2009-05-28 2012-06-29 Новартис Аг Замещенные производные аминомасляной кислоты в качестве ингибиторов неприлизина
DK2435409T3 (da) 2009-05-28 2014-10-27 Novartis Ag Substituerede aminopropionsyrederivater som neprilysininhibitorer
JO2967B1 (en) 2009-11-20 2016-03-15 نوفارتس ايه جي Acetic acid derivatives of carbamoyl methyl amino are substituted as new NEP inhibitors
CN104262228B (zh) 2010-01-22 2017-01-18 诺华股份有限公司 中性内肽酶抑制剂中间体和其制备方法
US8993631B2 (en) 2010-11-16 2015-03-31 Novartis Ag Method of treating contrast-induced nephropathy
US8673974B2 (en) 2010-11-16 2014-03-18 Novartis Ag Substituted amino bisphenyl pentanoic acid derivatives as NEP inhibitors
WO2012082857A1 (en) 2010-12-15 2012-06-21 Theravance, Inc. Neprilysin inhibitors
RU2622288C2 (ru) 2010-12-15 2017-06-14 ТЕРЕВАНС БАЙОФАРМА Ар энд Ди АйПи,ЭлЭлСи Ингибиторы неприлизина
ES2582640T3 (es) * 2011-02-17 2016-09-14 Theravance Biopharma R&D Ip, Llc Derivados aminobutíricos sustituidos como inhibidores de neprilisina
US8449890B2 (en) 2011-02-17 2013-05-28 Theravance, Inc. Neprilysin inhibitors
CA2835220A1 (en) 2011-05-31 2012-12-06 Theravance, Inc. Neprilysin inhibitors
CA2835216A1 (en) 2011-05-31 2012-12-06 Theravance, Inc. Neprilysin inhibitors
JP5885832B2 (ja) 2011-05-31 2016-03-16 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
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
WO2013184934A1 (en) 2012-06-08 2013-12-12 Theravance, Inc. Neprilysin inhibitors
US8871792B2 (en) 2012-06-08 2014-10-28 Theravance Biopharma R&D Ip, Llc Neprilysin inhibitors
KR102104954B1 (ko) * 2012-08-08 2020-04-27 세라밴스 바이오파마 알앤디 아이피, 엘엘씨 네프릴리신 억제제
EP3010914B1 (en) * 2013-06-19 2017-04-26 F. Hoffmann-La Roche AG Indolin-2-one or pyrrolo-pyridin/pyrimidin-2-one derivatives
EP3099678B1 (en) * 2014-01-30 2018-12-12 Theravance Biopharma R&D IP, LLC Neprilysin inhibitors
TWI731943B (zh) 2016-03-08 2021-07-01 美商施萬生物製藥研發Ｉｐ有限責任公司 結晶型（2s，4r）－5－（5’－氯－2’－氟－［1，1’－聯苯］－4－基）－2－（乙氧基甲基）－4－（3－羥基異㗁唑－5－甲醯胺基）－2－甲基戊酸及其用途

Also Published As

Publication number Publication date
US20210061776A1 (en) 2021-03-04
SA518392325B1 (ar) 2022-08-03
RU2018135072A3 (es) 2020-10-15
EP3408260B1 (en) 2021-05-05
RS62172B1 (sr) 2021-08-31
US20190002416A1 (en) 2019-01-03
AU2017229466B2 (en) 2020-08-13
PH12018501876A1 (en) 2019-01-28
PT3408260T (pt) 2021-07-23
DK3408260T3 (da) 2021-08-02
HRP20211169T1 (hr) 2021-11-12
ZA201805840B (en) 2019-07-31
US10100021B2 (en) 2018-10-16
RU2018135072A (ru) 2020-04-08
CO2018010568A2 (es) 2018-10-22
JP7306828B2 (ja) 2023-07-11
TW201741290A (zh) 2017-12-01
ES2880123T3 (es) 2021-11-23
US11230536B2 (en) 2022-01-25
WO2017156009A1 (en) 2017-09-14
US10472335B2 (en) 2019-11-12
SG11201807591VA (en) 2018-10-30
CY1124397T1 (el) 2022-07-22
RU2756223C2 (ru) 2021-09-28
AU2017229466A1 (en) 2018-09-13
CL2018002539A1 (es) 2018-10-26
PL3408260T3 (pl) 2021-11-08
US20170275259A1 (en) 2017-09-28
US10752599B2 (en) 2020-08-25
BR112018068170A2 (pt) 2019-01-29
IL261244B (en) 2022-02-01
JP2022017433A (ja) 2022-01-25
CN108779084A (zh) 2018-11-09
CA3015505A1 (en) 2017-09-14
US20200157061A1 (en) 2020-05-21
JP2019509286A (ja) 2019-04-04
HUE055546T2 (hu) 2021-12-28
EP3408260A1 (en) 2018-12-05
KR20180114225A (ko) 2018-10-17
KR20220035991A (ko) 2022-03-22
CA3015505C (en) 2024-03-05
LT3408260T (lt) 2021-07-26
US20220242836A1 (en) 2022-08-04
SI3408260T1 (sl) 2021-08-31
IL261244A (en) 2018-10-31
US11718591B2 (en) 2023-08-08
AU2017229466C1 (en) 2021-02-11
TWI731943B (zh) 2021-07-01

Similar Documents

Publication Publication Date Title
PH12018502747A1 (en) Boronic acid derivatives and therapeutic uses thereof
WO2017205536A3 (en) Heterocyclic inhibitors of cbp/ep300 and their use in the treatment of cancer
PH12015500780A1 (en) Rsv antiviral compounds
PH12017501397A1 (en) (2s, 4r)-5-(5`-chloro-2`-fluorobiphenyl-4-yl)-4-(ethoxyoxalylamino)-2-hydroxymethyl-2-methylpentanoic acid as neprilysin inhibitor
MX2015003653A (es) Derivados de amida del acido benzoimidazol-carboxilico como moduladores del receptor apj.
GEP201706748B (en) Heteroaromatic compounds as bruton's tyrosine kinase (btk) inhibitors
MX2020010300A (es) Sales monoacidas de 6-aminoisoquinolinas y usos de las mismas.
PH12015502365A1 (en) Bace1 inhibitors
MY167898A (en) Co-crystals and salts of ccr3-inhibitors
PH12017501444A1 (en) (2r,4r)-5-(5`-chloro-2`-fluorobiphenyl-4-yl)-2-hydroxy-4-[(5-methyloxazole-2-carbonyl)amino]pentanoic acid
PH12014502512A1 (en) Topical pharmaceutical compositions comprising terbinafine and urea
PH12018501876A1 (en) Crystalline(2s,4r)-5-(5'-chloro-2'-fluoro-[1,1'-biphenyl]-4-yl)-2-(ethoxymethyl)-4-(3-hydroxyisoxazole-5-carboxamido)-2-methylpentanoic acid and uses thereof
PH12014502541A1 (en) 5-amino [1,4] thiazines as bace 1 inhibitors
UA103329C2 (ru) Соли соединений-ингибиторов вич
UY37987A (es) Procedimiento para la preparación de (3s)-3-(4-cloro-3-{[(2s,3r)-2-(4-clorofenil)-4,4,4-trifluor-3- metilbutanoil]amino}fenil)-3-ácido ciclopropilpropanoico y su forma cristalina para uso como principio activo farmacéutico.
RU2013110517A (ru) Средство для профилактики или лечения неалкогольного стеатогепатита
IN2014MN02433A (es)
WO2012108794A3 (ru) Производные 1,2,4-триазол-з-илтиогликолевой кислоты для применения в терапии
WO2015036898A3 (en) Novel salts of crizotinib and their preparation
TN2013000150A1 (en) Co-crystals and salts of ccr3-inhibitors

Legal Events

Date Code Title Description
FG Grant or registration