ES2524784T3 - Formas polimórficas de un inhibidor macrocíclico del VHC - Google Patents

Formas polimórficas de un inhibidor macrocíclico del VHC Download PDF

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Publication number
ES2524784T3
ES2524784T3 ES08708575.9T ES08708575T ES2524784T3 ES 2524784 T3 ES2524784 T3 ES 2524784T3 ES 08708575 T ES08708575 T ES 08708575T ES 2524784 T3 ES2524784 T3 ES 2524784T3
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ES
Spain
Prior art keywords
hcv
polymorphic forms
macrocyclic inhibitor
macrocyclic
inhibitor
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Active
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ES08708575.9T
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English (en)
Inventor
Sigrid Carl Maria Stokbroekx
Carina Leys
Kelly Ann Swinney
Stijn Wuyts
Andras Horvath
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Janssen R&D Ireland ULC
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Janssen R&D Ireland ULC
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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • 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

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Molecular Biology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Steroid Compounds (AREA)

Abstract

Un compuesto de fórmula (I):**fórmula** en estado sólido, caracterizado por que está en forma cristalina.

Description

imagen1
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Tabla 6
Disolvente
Solubilidad de Forma I en g / 100 mL de disolución Solubilidad de Forma II en g / 100 mL de disolución
agua (pH = 5,0)
< 0,001 n.d.
metanol
0,056 0,29
etanol
0,050 0,17
2-propanol
0,027 0,11
2-propanona
0,66 1,2
tolueno
0,086 0,43
4-metil-2-pentanona
0,28 0,81
2-butanona
0,87 2,5
1-metoxi-2-propanol
0,82 1,6
acetonitrilo
0,075 0,20
1-butanol
n.d. 0,31
diclorometano
85 n.d.
acetato de etilo
0,21 n.d.
N,N-dimetilacetamida *
> 20 n.d.
N,N-dimetilacetamida
16 n.d.
tetrahidrofurano
7,0 n.d.
ácido acético
1,7 n.d.
ácido acético/agua (10/90) (v/v) (pH = 2,2)
< 0,001 n.d.
metanol/diclorometano (50/50) (v/v)
8,3 n.d.
2-propanol/diclorometano (97/3) (v/v)
0,045 0,19
etanol/agua (95/5) (v/v)
0,078 0,27
(*) 125 mg de Forma I se disolvieron en 0,5 mL de N,N-dimetilacetamida
n.d. = no determinada
25

Claims (1)

  1. imagen1
    imagen2
    imagen3
ES08708575.9T 2007-02-01 2008-02-01 Formas polimórficas de un inhibidor macrocíclico del VHC Active ES2524784T3 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP07101563 2007-02-01
EP07101563 2007-02-01
PCT/EP2008/051268 WO2008092954A2 (en) 2007-02-01 2008-02-01 Polymorphic forms of a macrocyclic inhibitor of hcv

Publications (1)

Publication Number Publication Date
ES2524784T3 true ES2524784T3 (es) 2014-12-12

Family

ID=38229348

Family Applications (1)

Application Number Title Priority Date Filing Date
ES08708575.9T Active ES2524784T3 (es) 2007-02-01 2008-02-01 Formas polimórficas de un inhibidor macrocíclico del VHC

Country Status (25)

Country Link
US (1) US8143402B2 (es)
EP (1) EP2118098B1 (es)
JP (1) JP5523110B2 (es)
KR (1) KR101580226B1 (es)
CN (3) CN105037347B (es)
AR (2) AR065136A1 (es)
AU (1) AU2008209696B2 (es)
BR (1) BRPI0806945A2 (es)
CA (1) CA2677170C (es)
CL (1) CL2008000321A1 (es)
CY (1) CY1116339T1 (es)
DK (1) DK2118098T3 (es)
ES (1) ES2524784T3 (es)
HK (1) HK1205125A1 (es)
HR (1) HRP20141137T1 (es)
IL (1) IL199215A (es)
MX (1) MX2009008275A (es)
NZ (1) NZ577568A (es)
PL (1) PL2118098T3 (es)
PT (1) PT2118098E (es)
RU (1) RU2533830C2 (es)
SI (1) SI2118098T1 (es)
TW (1) TWI423968B (es)
WO (1) WO2008092954A2 (es)
ZA (1) ZA200905377B (es)

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MY140680A (en) 2002-05-20 2010-01-15 Bristol Myers Squibb Co Hepatitis c virus inhibitors
PE20070211A1 (es) 2005-07-29 2007-05-12 Medivir Ab Compuestos macrociclicos como inhibidores del virus de hepatitis c
US8207341B2 (en) 2008-09-04 2012-06-26 Bristol-Myers Squibb Company Process or synthesizing substituted isoquinolines
UY32099A (es) 2008-09-11 2010-04-30 Enanta Pharm Inc Inhibidores macrocíclicos de serina proteasas de hepatitis c
PL2401272T3 (pl) * 2009-02-27 2017-06-30 Janssen Pharmaceuticals, Inc. Amorficzna sól makrocyklicznego inhibitora HCV
TW201040181A (en) 2009-04-08 2010-11-16 Idenix Pharmaceuticals Inc Macrocyclic serine protease inhibitors
EP2461811B1 (en) 2009-08-05 2016-04-20 Idenix Pharmaceuticals LLC. Macrocyclic serine protease inhibitors useful against viral infections, particularly hcv
KR101781789B1 (ko) 2010-01-27 2017-09-26 에이비 파르마 리미티드. C형 간염 바이러스 억제제로 사용되는 다환 헤테로사이클릭 화합물
EP2658859A4 (en) 2010-12-30 2014-07-30 Enanta Pharm Inc MACROCYCLIC HEPATITIS C SERIN PROTEASE INHIBITORS
KR20140003521A (ko) 2010-12-30 2014-01-09 이난타 파마슈티칼스, 인코포레이티드 페난트리딘 매크로사이클릭 ｃ형 간염 세린 프로테아제 억제제
AR085352A1 (es) 2011-02-10 2013-09-25 Idenix Pharmaceuticals Inc Inhibidores macrociclicos de serina proteasa, sus composiciones farmaceuticas y su uso para tratar infecciones por hcv
CN103501608A (zh) * 2011-05-04 2014-01-08 默沙东公司 药用物质、药物组合物和制备它们的方法
US8957203B2 (en) 2011-05-05 2015-02-17 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
US10201584B1 (en) 2011-05-17 2019-02-12 Abbvie Inc. Compositions and methods for treating HCV
US8691757B2 (en) 2011-06-15 2014-04-08 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
CA2857705A1 (en) 2011-06-16 2012-12-20 AB Pharma Ltd. Macrocyclic heterocyclic compounds for inhibiting hepatitis c virus and preparation and use thereof
BR112014005935A2 (pt) 2011-09-16 2017-03-28 Fovea Pharmaceuticals derivados de anilina, sua preparação e sua aplicação terapêutica
DE112012002748T5 (de) 2011-10-21 2014-07-31 Abbvie Inc. Verfahren zur Behandlung von HCV umfassend mindestens zwei direkt wirkende antivirale Wirkstoffe, Ribavirin aber nicht Interferon
US8492386B2 (en) 2011-10-21 2013-07-23 Abbvie Inc. Methods for treating HCV
US8466159B2 (en) 2011-10-21 2013-06-18 Abbvie Inc. Methods for treating HCV
SE1450131A1 (sv) 2011-10-21 2014-05-07 Abbvie Inc DAA-kombinationsbehandling (t.ex. med ABT-072 eller ABT-333)för användning vid behandling av HCV
EA025560B1 (ru) 2012-10-19 2017-01-30 Бристол-Майерс Сквибб Компани Ингибиторы вируса гепатита с
WO2014070964A1 (en) 2012-11-02 2014-05-08 Bristol-Myers Squibb Company Hepatitis c virus inhibitors
WO2014071007A1 (en) 2012-11-02 2014-05-08 Bristol-Myers Squibb Company Hepatitis c virus inhibitors
US9643999B2 (en) 2012-11-02 2017-05-09 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
EP2914614B1 (en) 2012-11-05 2017-08-16 Bristol-Myers Squibb Company Hepatitis c virus inhibitors
WO2014137869A1 (en) 2013-03-07 2014-09-12 Bristol-Myers Squibb Company Hepatitis c virus inhibitors
EP3089757A1 (en) 2014-01-03 2016-11-09 AbbVie Inc. Solid antiviral dosage forms
WO2015109925A1 (zh) * 2014-01-21 2015-07-30 杭州普晒医药科技有限公司 丙型肝炎药物的晶型及其制备方法、其药物组合物和用途
CN105308043B (zh) * 2014-05-29 2018-01-30 杭州普晒医药科技有限公司 丙型肝炎药物的晶型及其制备方法、其药物组合物和用途
CZ2015220A3 (cs) * 2015-03-27 2016-10-05 Zentiva, K.S. Amorfní sůl makrocyklického inhibitoru viru hepatitidy C
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CN105503851B (zh) * 2015-12-09 2017-06-23 重庆润生科技有限公司 一种烯基噻唑衍生物的制备方法
EA201892448A1 (ru) 2016-04-28 2019-06-28 Эмори Юниверсити Алкинсодержащие нуклеотидные и нуклеозидные терапевтические композиции и связанные с ними способы применения

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CA2515216A1 (en) * 2003-02-07 2004-08-26 Enanta Pharmaceuticals, Inc. Macrocyclic hepatitis c serine protease inhibitors
JP4525982B2 (ja) * 2003-09-26 2010-08-18 シェーリング コーポレイション Ｃ型肝炎ウイルスのｎｓ３セリンプロテアーゼの大環状インヒビター
HRP20130098T1 (hr) * 2003-10-14 2013-02-28 F. Hoffmann - La Roche Ag MAKROCIKLIÄŚKE KARBOKSILNE KISELINE I ACILSULFONAMIDNI SPOJEVI KAO INHIBITORI REPLIKACIJE HCV-a
PL1713822T3 (pl) * 2004-01-30 2010-08-31 Medivir Ab Inhibitory proteazy serynowej HCV NS-3
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Also Published As

Publication number Publication date
RU2009132660A (ru) 2011-03-10
EP2118098A2 (en) 2009-11-18
HK1137438A1 (en) 2010-07-30
CA2677170A1 (en) 2008-08-07
ZA200905377B (en) 2010-10-27
DK2118098T3 (en) 2014-12-08
HRP20141137T1 (hr) 2015-01-30
KR101580226B1 (ko) 2015-12-24
WO2008092954A2 (en) 2008-08-07
CN105037347B (zh) 2018-06-01
NZ577568A (en) 2012-02-24
CA2677170C (en) 2017-04-18
CN105037347A (zh) 2015-11-11
AU2008209696B2 (en) 2013-05-09
TWI423968B (zh) 2014-01-21
EP2118098B1 (en) 2014-09-24
HK1205125A1 (en) 2015-12-11
IL199215A (en) 2015-10-29
CL2008000321A1 (es) 2008-08-22
PL2118098T3 (pl) 2015-03-31
CN104230918B (zh) 2018-01-26
US20100029715A1 (en) 2010-02-04
JP2010517971A (ja) 2010-05-27
BRPI0806945A2 (pt) 2014-05-06
CY1116339T1 (el) 2017-02-08
CN101589040A (zh) 2009-11-25
CN104230918A (zh) 2014-12-24
WO2008092954A8 (en) 2009-12-23
AU2008209696A1 (en) 2008-08-07
AR108819A2 (es) 2018-09-26
AR065136A1 (es) 2009-05-20
SI2118098T1 (sl) 2015-01-30
US8143402B2 (en) 2012-03-27
RU2533830C2 (ru) 2014-11-20
WO2008092954A3 (en) 2008-10-02
MX2009008275A (es) 2009-08-12
KR20090115929A (ko) 2009-11-10
PT2118098E (pt) 2014-12-09
TW200846347A (en) 2008-12-01
JP5523110B2 (ja) 2014-06-18

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