AR092121A1 - Formas solidas de un compuesto antiviral - Google Patents

Formas solidas de un compuesto antiviral

Info

Publication number
AR092121A1
AR092121A1 ARP130102877A ARP130102877A AR092121A1 AR 092121 A1 AR092121 A1 AR 092121A1 AR P130102877 A ARP130102877 A AR P130102877A AR P130102877 A ARP130102877 A AR P130102877A AR 092121 A1 AR092121 A1 AR 092121A1
Authority
AR
Argentina
Prior art keywords
compound
solid forms
antiviral compound
dimethylbutin
methylcyclohex
Prior art date
Application number
ARP130102877A
Other languages
English (en)
Inventor
Wolckenhauer Scott
Shi Bing
Hashash Ahmad
Original Assignee
Gilead Sciences Inc
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 Gilead Sciences Inc filed Critical Gilead Sciences Inc
Publication of AR092121A1 publication Critical patent/AR092121A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
    • A61K31/381—Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
    • 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
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/7056—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing five-membered rings with nitrogen as a ring hetero atom
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7068—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
    • A61K31/7072—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
    • 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
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
    • C07D407/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/08—Bridged systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (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)

Abstract

Se prepararon formas cristalinas sólidas y la forma amorfa del compuesto anti-VHC ácido 5-(3,3-dimetilbutin-1-il)-3-[(cis-4-hidroxi-4-{[(3S)-tetrahidrofurano-3-iloxi]metil}ciclohexil){[(1R)-4-metilciclohex-3-en-1-il]carbonil}amino]tiofeno-2-carboxílico (Compuesto 1) y se caracterizaron en estado sólido. También, procesos para su fabricación y métodos para utilizar las formas cristalinas. Compuesto útil para utilizar en el tratamiento de la hepatitis C. Reivindicación 1: Un hidrato cristalino del ácido 5-(3,3-dimetilbutin-1-il)-3-[(cis-4-hidroxi-4-{[(3S)-tetrahidrofurano-3-iloxi]metil}ciclohexil){[(1R)-4-metilciclohex-3-en-1-il]carbonil}amino]tiofeno-2-carboxílico (Compuesto 1, Forma I) caracterizado porque tiene un difractograma de rayos X en polvo que comprende por lo menos tres de los siguientes picos: 4,0, 7,3, 8,1, 17,9, ó 21,8 º2q ± 0,2 º2q, determinado en un difractómetro usando radiación Cu-Ka.
ARP130102877A 2012-08-17 2013-08-13 Formas solidas de un compuesto antiviral AR092121A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201261684297P 2012-08-17 2012-08-17
US13/800,991 US8841340B2 (en) 2012-08-17 2013-03-13 Solid forms of an antiviral compound

Publications (1)

Publication Number Publication Date
AR092121A1 true AR092121A1 (es) 2015-03-25

Family

ID=50100473

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP130102877A AR092121A1 (es) 2012-08-17 2013-08-13 Formas solidas de un compuesto antiviral

Country Status (10)

Country Link
US (2) US8841340B2 (es)
EP (1) EP2885295A1 (es)
JP (2) JP2015524840A (es)
AR (1) AR092121A1 (es)
AU (1) AU2013302914C1 (es)
CA (1) CA2882119A1 (es)
HK (1) HK1211924A1 (es)
TW (1) TW201420586A (es)
UY (1) UY34976A (es)
WO (1) WO2014028343A1 (es)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2345657A1 (en) 2003-05-30 2011-07-20 Pharmasset, Inc. Modified fluorinated nucleoside analogues
PE20091163A1 (es) * 2007-11-01 2009-08-09 Wyeth Corp Anticuerpos para gdf8
ME02536B (me) * 2009-05-13 2017-02-20 Gilead Pharmasset Llc Antiviralna jedinjenja
US8841340B2 (en) 2012-08-17 2014-09-23 Gilead Sciences, Inc. Solid forms of an antiviral compound
US8759544B2 (en) 2012-08-17 2014-06-24 Gilead Sciences, Inc. Synthesis of an antiviral compound
EP2950786B1 (en) 2013-01-31 2019-11-27 Gilead Pharmasset LLC Combination formulation of two antiviral compounds
PL3038601T3 (pl) 2013-08-27 2020-08-24 Gilead Pharmasset Llc Formulacja złożona dwóch związków przeciwwirusowych
CN104974205A (zh) * 2014-09-19 2015-10-14 苏州晶云药物科技有限公司 索非布韦的晶型a及其制备方法
EP3939985B1 (en) 2014-12-26 2024-05-08 Emory University Pharmaceutical compositions comprising n4-hydroxycytidine derivatives for the treatment or prevention of influenza or coronavirus infections
ES2938859T3 (es) * 2017-05-01 2023-04-17 Gilead Sciences Inc Una forma cristalina de (S)-2-etilbutilo 2-(((S)-(((2R,3S,4R,5R)-5-(4-aminopirrolo[2,1-f][1,2,4]triazin-7-il)-5-ciano-3,4-dihidroxitetrahidrofuran-2-il)metoxi)(fenoxi)fosforil)amino)propanoato
KR102626210B1 (ko) 2017-12-07 2024-01-18 에모리 유니버시티 N4-하이드록시사이티딘 및 유도체 및 이와 관련된 항-바이러스 용도
CA3220903A1 (en) 2021-05-21 2022-11-24 Gilead Sciences, Inc. Pentacyclic derivatives as zika virus inhibitors

Family Cites Families (36)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3845770A (en) 1972-06-05 1974-11-05 Alza Corp Osmatic dispensing device for releasing beneficial agent
US4326525A (en) 1980-10-14 1982-04-27 Alza Corporation Osmotic device that improves delivery properties of agent in situ
US5364620A (en) 1983-12-22 1994-11-15 Elan Corporation, Plc Controlled absorption diltiazem formulation for once daily administration
US5023252A (en) 1985-12-04 1991-06-11 Conrex Pharmaceutical Corporation Transdermal and trans-membrane delivery of drugs
US5001139A (en) 1987-06-12 1991-03-19 American Cyanamid Company Enchancers for the transdermal flux of nivadipine
US4992445A (en) 1987-06-12 1991-02-12 American Cyanamid Co. Transdermal delivery of pharmaceuticals
US4902514A (en) 1988-07-21 1990-02-20 Alza Corporation Dosage form for administering nilvadipine for treating cardiovascular symptoms
US5861421A (en) 1995-12-21 1999-01-19 Smithkline Beecham Corporation 4,4-(disubstituted) cyclohexan-1-one monomers and related compounds
US20050119332A1 (en) 1998-03-12 2005-06-02 Lone Jeppesen Substituted thiophene compounds as modulators of protein tyrosine phosphatases (PTPases)
US20020002199A1 (en) 1998-03-12 2002-01-03 Lone Jeppesen Modulators of protein tyrosine phosphatases (ptpases)
CN101624391A (zh) 2001-06-11 2010-01-13 病毒化学医药公司 用作黄病毒感染抗病毒剂的噻吩衍生物
US6887877B2 (en) 2001-06-11 2005-05-03 Virochem Pharma Inc. Compounds and methods for the treatment or prevention of Flavivirus infections
CN100413861C (zh) 2002-12-10 2008-08-27 维勒凯姆制药股份有限公司 用于治疗或预防黄病毒感染的化合物
MXPA05006196A (es) 2002-12-10 2006-01-27 Virochem Pharma Inc Compuestos y metodos para el tratamiento o prevencion de infecciones por flavivirus.
US20050052161A1 (en) 2003-09-08 2005-03-10 Scamard David Franklin Instant charge battery
DE10359791A1 (de) 2003-12-19 2005-07-21 Bayer Healthcare Ag Substituierte Thiophene
TW200602337A (en) 2004-02-25 2006-01-16 Wyeth Corp Inhibitors of protein tyrosine phosphatase 1B
US7470701B2 (en) 2004-03-30 2008-12-30 Novartis Vaccines And Diagnostics, Inc. Substituted 2,5-heterocyclic derivatives
DE102005028077A1 (de) 2004-12-22 2006-07-13 Aicuris Gmbh & Co. Kg Alkinyl-substituierte Thiophene
DE102004061746A1 (de) 2004-12-22 2006-07-06 Bayer Healthcare Ag Alkinyl-substituierte Thiophene
EP2546246A3 (en) 2005-05-13 2013-04-24 Virochem Pharma Inc. Compounds and methods for the treatment or prevention of flavivirus infections
KR20080096670A (ko) 2006-02-15 2008-10-31 사노피-아벤티스 신규한 아미노 알콜-치환된 아릴티에노피리미디논, 이의 제조 방법 및 약제로서 이의 용도
EA201101492A1 (ru) 2006-11-15 2012-09-28 Вирокем Фарма Инк. Аналоги тиофена для лечения или предупреждения флавивирусных инфекций
JP2010510191A (ja) 2006-11-17 2010-04-02 スミスクライン ビーチャム コーポレーション 抗ウイルス剤としての２−カルボキシチオフェン誘導体
EA201190007A1 (ru) 2008-12-03 2012-06-29 Пресидио Фармасьютикалс, Инк. Ингибиторы ns5a вгс
EA020816B1 (ru) 2009-07-21 2015-01-30 Джилид Сайэнс, Инк. Ингибиторы вирусов flaviviridae
JP5774008B2 (ja) 2009-09-09 2015-09-02 ギリアード サイエンシーズ， インコーポレイテッド Ｆｌａｖｉｖｉｒｉｄａｅウイルスの阻害剤
WO2011068715A1 (en) 2009-11-25 2011-06-09 Vertex Pharmaceuticals Incorporated 5-alkynyl-thiophene-2-carboxylic acid derivatives and their use for the treatment or prevention of flavivirus infections
PL2523950T3 (pl) 2010-01-15 2017-09-29 Gilead Sciences, Inc. Inhibitory wirusów flaviviridae
KR20120123678A (ko) 2010-01-15 2012-11-09 길리애드 사이언시즈, 인코포레이티드 플라비비리다에 바이러스의 억제제
AU2011276526A1 (en) 2010-06-28 2013-01-10 Vertex Pharmaceuticals Incorporated Compounds and methods for the treatment or prevention of Flavivirus infections
TW201306841A (zh) 2010-12-20 2013-02-16 Gilead Sciences Inc 治療ｃ型肝炎病毒（ｈｃｖ）之方法
ES2561888T3 (es) 2011-07-13 2016-03-01 Gilead Sciences, Inc. Derivados de ácido tiofeno-2-carboxílico útiles como inhibidores de virus Flaviviridae
US8759544B2 (en) 2012-08-17 2014-06-24 Gilead Sciences, Inc. Synthesis of an antiviral compound
US8841340B2 (en) 2012-08-17 2014-09-23 Gilead Sciences, Inc. Solid forms of an antiviral compound
US8927741B2 (en) 2012-08-17 2015-01-06 Gilead Sciences, Inc. Synthesis of an antiviral compound

Also Published As

Publication number Publication date
TW201420586A (zh) 2014-06-01
AU2013302914B2 (en) 2017-08-10
HK1211924A1 (en) 2016-06-03
UY34976A (es) 2014-02-28
JP2018162278A (ja) 2018-10-18
AU2013302914C1 (en) 2018-05-17
CA2882119A1 (en) 2014-02-20
AU2013302914A1 (en) 2015-02-05
EP2885295A1 (en) 2015-06-24
WO2014028343A1 (en) 2014-02-20
US8841340B2 (en) 2014-09-23
US9409891B2 (en) 2016-08-09
US20140051749A1 (en) 2014-02-20
JP2015524840A (ja) 2015-08-27
US20140309187A1 (en) 2014-10-16

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