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
Prior art date
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Active
Application number
ES08708575.9T
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English (en)
Inventor
Sigrid Carl Maria Stokbroekx
Carina Leys
Kelly Ann Swinney
Stijn Wuyts
Andras Horvath
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Janssen R&D Ireland ULC
Original Assignee
Janssen R&D Ireland ULC
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Filing date
Publication date
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Application filed by Janssen R&D Ireland ULC filed Critical 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

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) CN104230918B (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 (2) HK1137438A1 (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)

Families Citing this family (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
SI2401272T1 (sl) * 2009-02-27 2017-04-26 Janssen Pharmaceuticals, Inc. Amorfna sol makrocikličnega inhibitorja VHC
EP2417134B1 (en) 2009-04-08 2017-05-17 Idenix Pharmaceuticals LLC. Macrocyclic serine protease inhibitors
WO2011017389A1 (en) 2009-08-05 2011-02-10 Idenix Pharmaceuticals, Inc. Macrocyclic serine protease inhibitors useful against viral infections, particularly hcv
CA2788155C (en) 2010-01-27 2018-04-24 AB Pharma Ltd. Polyheterocyclic compounds highly potent as hcv inhibitors
AU2011352145A1 (en) 2010-12-30 2013-07-18 Abbvie Inc. Phenanthridine macrocyclic hepatitis C serine protease inhibitors
WO2012092409A2 (en) 2010-12-30 2012-07-05 Enanta Phararmaceuticals, Inc Macrocyclic hepatitis c serine protease inhibitors
WO2012109398A1 (en) 2011-02-10 2012-08-16 Idenix Pharmaceuticals, Inc. Macrocyclic serine protease inhibitors, pharmaceutical compositions thereof, and their use for treating hcv infections
JP2014515764A (ja) * 2011-05-04 2014-07-03 メルク・シャープ・アンド・ドーム・コーポレーション Ｃ型肝炎ウイルス阻害剤の調製法
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
WO2012171332A1 (zh) 2011-06-16 2012-12-20 爱博新药研发(上海)有限公司 抑制丙型肝炎病毒的大环状杂环化合物及其制备和应用
AU2012307527B2 (en) 2011-09-16 2017-07-20 Sanofi Aniline derivatives,their preparation and their therapeutic application
US8466159B2 (en) 2011-10-21 2013-06-18 Abbvie Inc. Methods for treating HCV
US8492386B2 (en) 2011-10-21 2013-07-23 Abbvie Inc. Methods for treating HCV
WO2013059630A1 (en) 2011-10-21 2013-04-25 Abbvie Inc. Methods for treating hcv comprising at least two direct acting antiviral agent, ribavirin but not interferon.
PT107924A (pt) 2011-10-21 2014-12-03 Abbvie Inc Tratamento de combinação de daa (eg. com abt-072 ou abt-333) para utilização no tratamento de hcv
KR20150074051A (ko) 2012-10-19 2015-07-01 브리스톨-마이어스 스큅 컴퍼니 C형 간염 바이러스 억제제
US9334279B2 (en) 2012-11-02 2016-05-10 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
US9643999B2 (en) 2012-11-02 2017-05-09 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
WO2014070964A1 (en) 2012-11-02 2014-05-08 Bristol-Myers Squibb Company Hepatitis c virus inhibitors
US9409943B2 (en) 2012-11-05 2016-08-09 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
WO2016177625A1 (en) 2015-05-04 2016-11-10 Sandoz Ag Amorphous simeprevir potassium
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
WO2017189978A1 (en) 2016-04-28 2017-11-02 Emory University Alkyne containing nucleotide and nucleoside therapeutic compositions and uses related thereto

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2007524576A (ja) * 2003-02-07 2007-08-30 エナンタ ファーマシューティカルズ インコーポレイテッド 大環状のｃ型肝炎セリンプロテアーゼ阻害剤
TWI280964B (en) * 2003-09-26 2007-05-11 Schering Corp Macrocyclic inhibitors of hepatitis C virus NS3 serine protease
BRPI0415373A (pt) * 2003-10-14 2006-12-12 Intermune Inc ácidos carboxìlicos macrocìclicos e acilsulfonamidas como inibidores de replicação de hcv
JP4902361B2 (ja) * 2004-01-30 2012-03-21 メディヴィル・アクチエボラーグ Ｈｃｖｎｓ−３セリンプロテアーゼインヒビター
PE20070211A1 (es) 2005-07-29 2007-05-12 Medivir Ab Compuestos macrociclicos como inhibidores del virus de hepatitis c

Also Published As

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

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