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PE20040767A1 - Derivado hemisulfato de azido citosina cristalino anhidro - Google Patents

Derivado hemisulfato de azido citosina cristalino anhidro

Info

Publication number
PE20040767A1
PE20040767A1 PE2003001233A PE2003001233A PE20040767A1 PE 20040767 A1 PE20040767 A1 PE 20040767A1 PE 2003001233 A PE2003001233 A PE 2003001233A PE 2003001233 A PE2003001233 A PE 2003001233A PE 20040767 A1 PE20040767 A1 PE 20040767A1
Authority
PE
Peru
Prior art keywords
refers
hemisulphate
anhydro
crystalline
derivative
Prior art date
Application number
PE2003001233A
Other languages
English (en)
Inventor
Joseph Armstrong Martin
Anthony Prince
Keshab Sarma
Terrence Joseph Connolly
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of PE20040767A1 publication Critical patent/PE20040767A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/06—Pyrimidine radicals
    • 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
    • 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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • Genetics & Genomics (AREA)
  • Communicable Diseases (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
  • Steroid Compounds (AREA)

Abstract

SE REFIERE A LA SAL HEMISULFATO DE 1-[4(S)-AZIDO-2(S),3(R)-DIHIDROXI-4-(HIDROXIMETIL)-1(R)-CICLOPENTIL]CITOSINA DE FORMULA (Ia) QUE PRESENTA UNA MAYOR ESTABILIDAD Y MEJORES PROPIEDADES FISICAS, DICHA SAL DE HEMISULFATO PRESENTA 3 FORMAS CRISTALINAS POLIMORFICAS. LA FORMA A CON UNA HUELLA DE DIFRACCION DE POLVO POR RAYOS X ,TIENEN UNA DISTANCIAS D CON UN RANGO DE 17.5556 A 2.9787, LA FORMA B TIENE UN RANGO DE 2.8037 A 2.6227 Y LA FORMA C DE 7.7865 A 2.7752. TAMBIEN SE REFIERE A UN PROCEDIMIENTO PARA LA PREPARACION DE ESTAS SALES, QUE COMPRENDE LA CRISTALIZACION DEL COMPUESTO A PARTIR DE UNA SOLUCION ENVEJECIDA DE ACIDO SULFURICO EN ETANOL PARA LA FORMA A, UNA SOLUCION DE ISOPROPANOL/AGUA (85:15) PARA LA FORMA B Y (60:40) PARA LA FORMA C, AMBAS EN PRESENCIA DE ACIDO SULFURICO. ADEMAS SE REFIERE A UNA COMPOSICION FARMACEUTICA QUE LO CONTIENE Y A UN METODO PARA EL TRATAMIENTO DE UNA ENFERMEDAD INDUCIDA POR EL VIRUS DE LA HEPATITIS C
PE2003001233A 2002-12-09 2003-12-05 Derivado hemisulfato de azido citosina cristalino anhidro PE20040767A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US43188502P 2002-12-09 2002-12-09

Publications (1)

Publication Number Publication Date
PE20040767A1 true PE20040767A1 (es) 2004-11-06

Family

ID=32507815

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2003001233A PE20040767A1 (es) 2002-12-09 2003-12-05 Derivado hemisulfato de azido citosina cristalino anhidro

Country Status (32)

Country Link
US (1) US6864244B2 (es)
EP (1) EP1572711B1 (es)
JP (1) JP4563818B2 (es)
KR (1) KR100675544B1 (es)
CN (1) CN1314697C (es)
AR (1) AR042312A1 (es)
AT (1) ATE430755T1 (es)
AU (1) AU2003292212B2 (es)
BR (1) BR0317146A (es)
CA (1) CA2506532C (es)
CY (1) CY1109296T1 (es)
DE (1) DE60327554D1 (es)
DK (1) DK1572711T3 (es)
ES (1) ES2324654T3 (es)
GT (1) GT200300276A (es)
HR (1) HRP20050503A2 (es)
IL (1) IL168685A (es)
JO (1) JO2542B1 (es)
MX (1) MXPA05006044A (es)
MY (1) MY130927A (es)
NO (1) NO330454B1 (es)
NZ (1) NZ540297A (es)
PA (1) PA8590701A1 (es)
PE (1) PE20040767A1 (es)
PL (1) PL213734B1 (es)
PT (1) PT1572711E (es)
RU (1) RU2334756C2 (es)
SI (1) SI1572711T1 (es)
TW (1) TWI294882B (es)
UY (1) UY28109A1 (es)
WO (1) WO2004052906A1 (es)
ZA (1) ZA200504472B (es)

Families Citing this family (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP4577751B2 (ja) * 1999-09-02 2010-11-10 塩野義製薬株式会社 芳香族ヘテロ環誘導体を含有するインテグラーゼ阻害剤
CA2284459C (en) 1999-10-04 2012-12-11 Neokimia Inc. Combinatorial synthesis of libraries of macrocyclic compounds useful in drug discovery
US20050182252A1 (en) * 2004-02-13 2005-08-18 Reddy K. R. Novel 2'-C-methyl nucleoside derivatives
DE602005015466D1 (de) * 2004-08-23 2009-08-27 Hoffmann La Roche Antivirale 4'-azidonucleoside
SI2084175T1 (sl) * 2006-10-10 2011-05-31 Medivir Ab Hcv nukleozidni inhibitor
JP2010515680A (ja) 2007-01-05 2010-05-13 メルク・シャープ・エンド・ドーム・コーポレイション Ｒｎａ依存性ｒｎａウイルス感染症の治療用としてのヌクレオシドアリールホスホロアミデート
GB0709791D0 (en) * 2007-05-22 2007-06-27 Angeletti P Ist Richerche Bio Antiviral agents
GB0900914D0 (en) 2009-01-20 2009-03-04 Angeletti P Ist Richerche Bio Antiviral agents
CA2812962C (en) 2010-09-22 2020-03-31 Alios Biopharma, Inc. Azido nucleosides and nucleotide analogs
CA2937548C (en) 2014-02-13 2022-10-25 Ligand Pharmaceuticals, Inc. Prodrug compounds and their uses
CN103965116B (zh) * 2014-05-06 2016-06-15 中国科学院苏州纳米技术与纳米仿生研究所 半5-氟胞嘧啶盐、其制备方法及应用
WO2016003812A1 (en) 2014-07-02 2016-01-07 Ligand Pharmaceuticals, Inc. Prodrug compounds and uses therof
GEP20237502B (en) 2015-03-06 2023-04-25 Atea Pharmaceuticals Inc B-D-2'-DEOXY-2'a-FLUORO-2'-B-C-SUBSTITUTED-2-MODIFIED-N6-SUBSTITUTED PURINE NUCLEOTIDES FOR HCV TREATMENT
EA202190602A3 (ru) 2016-09-07 2021-11-30 Атеа Фармасьютикалс, Инк. 2'-замещенные-n6-замещенные пуриновые нуклеотиды для лечения вызванных рнк-вирусом заболеваний
GEP20237457B (en) 2017-02-01 2023-01-10 Atea Pharmaceuticals Inc Nucleotide hemi-sulfate salt for treatment of hepatitis c virus
AU2019207625A1 (en) 2018-01-09 2020-07-30 Ligand Pharmaceuticals, Inc. Acetal compounds and therapeutic uses thereof
JP2021521118A (ja) 2018-04-10 2021-08-26 アテア ファーマシューティカルズ， インコーポレイテッド 肝硬変を伴うｈｃｖ感染患者の治療
US10874687B1 (en) 2020-02-27 2020-12-29 Atea Pharmaceuticals, Inc. Highly active compounds against COVID-19
KR20240022574A (ko) 2021-06-17 2024-02-20 아테아 파마슈티컬즈, 인크. 유리한 항-hcv 조합 요법
CN115536710B (zh) * 2022-10-18 2024-04-16 南京工业大学 一种高品质胞苷硫酸盐晶体的制备方法

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5449664A (en) * 1988-11-21 1995-09-12 Syntex (U.S.A.) Inc. Antiviral agents
PH27609A (en) * 1988-11-21 1993-08-31 Syntex Inc Antiviral agents
AU7623991A (en) * 1990-05-17 1991-11-21 Syntex (U.S.A.) Inc. Antiviral agents
PT1027359E (pt) * 1996-10-16 2003-09-30 Ribapharm Inc L-nucleosideos monociclicos analogos e suas utilizacoes
US20030008841A1 (en) * 2000-08-30 2003-01-09 Rene Devos Anti-HCV nucleoside derivatives
SI1355916T1 (sl) * 2001-01-22 2007-04-30 Merck & Co Inc Nukleozidni derivati kot inhibitorji RNA-odvisne RNA virusne polimeraze
GB0114286D0 (en) * 2001-06-12 2001-08-01 Hoffmann La Roche Nucleoside Derivatives

Also Published As

Publication number Publication date
AU2003292212B2 (en) 2009-10-01
NO330454B1 (no) 2011-04-18
HRP20050503A2 (en) 2006-12-31
HK1085483A1 (en) 2006-08-25
JO2542B1 (en) 2010-09-05
AU2003292212A1 (en) 2004-06-30
DK1572711T3 (da) 2009-07-13
TWI294882B (en) 2008-03-21
CY1109296T1 (el) 2014-07-02
WO2004052906A1 (en) 2004-06-24
CN1723215A (zh) 2006-01-18
PA8590701A1 (es) 2004-11-26
NO20052732D0 (no) 2005-06-07
CA2506532C (en) 2011-09-20
UY28109A1 (es) 2004-06-30
KR20050084217A (ko) 2005-08-26
MY130927A (en) 2007-07-31
NZ540297A (en) 2007-05-31
CN1314697C (zh) 2007-05-09
US6864244B2 (en) 2005-03-08
KR100675544B1 (ko) 2007-01-30
MXPA05006044A (es) 2005-08-18
JP4563818B2 (ja) 2010-10-13
GT200300276A (es) 2004-09-02
RU2005121927A (ru) 2006-01-27
RU2334756C2 (ru) 2008-09-27
ATE430755T1 (de) 2009-05-15
ES2324654T3 (es) 2009-08-12
ZA200504472B (en) 2006-02-22
DE60327554D1 (de) 2009-06-18
NO20052732L (no) 2005-09-06
AR042312A1 (es) 2005-06-15
PL377472A1 (pl) 2006-02-06
PL213734B1 (pl) 2013-04-30
US20040162265A1 (en) 2004-08-19
EP1572711B1 (en) 2009-05-06
SI1572711T1 (sl) 2009-08-31
TW200502243A (en) 2005-01-16
CA2506532A1 (en) 2004-06-24
PT1572711E (pt) 2009-06-25
EP1572711A1 (en) 2005-09-14
BR0317146A (pt) 2005-10-25
IL168685A (en) 2010-11-30
JP2006510649A (ja) 2006-03-30

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Legal Events

Date Code Title Description
FG Grant, registration
FD Application declared void or lapsed