UY32642A - Espironucleósidos uracílicos oxetánicos - Google Patents

Espironucleósidos uracílicos oxetánicos

Info

Publication number
UY32642A
UY32642A UY0001032642A UY32642A UY32642A UY 32642 A UY32642 A UY 32642A UY 0001032642 A UY0001032642 A UY 0001032642A UY 32642 A UY32642 A UY 32642A UY 32642 A UY32642 A UY 32642A
Authority
UY
Uruguay
Prior art keywords
phenyl
alkyl
optionally substituted
spironucleosids
oxethanic
Prior art date
Application number
UY0001032642A
Other languages
English (en)
Inventor
Van Hoof Steven Maurice Paula
Jonckers Tim Hugo Maria
Raboisson Pierre Jean-Marie Bernard
Vandyck Koen
Hu Lili
Tahri Abdellah
Original Assignee
Medivir Ab
Centocor Ortho Biotech Products L P
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 Medivir Ab, Centocor Ortho Biotech Products L P filed Critical Medivir Ab
Publication of UY32642A publication Critical patent/UY32642A/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
    • C07H19/10—Pyrimidine radicals with the saccharide radical esterified by phosphoric or polyphosphoric acids
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/503—Pyridazines; Hydrogenated pyridazines spiro-condensed
    • 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
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • C07H15/02—Acyclic radicals, not substituted by cyclic structures
    • C07H15/04—Acyclic radicals, not substituted by cyclic structures attached to an oxygen atom of the saccharide radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • C07H15/18—Acyclic radicals, substituted by carbocyclic rings
    • 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
    • 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
    • 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
    • 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
    • C07H19/067—Pyrimidine radicals with ribosyl as the saccharide radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H21/00—Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids
    • C07H21/02—Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids with ribosyl as saccharide radical

Abstract

Compuestos de la fórmula I incluyendo cualquier estereoisómero posible de los mismos, en donde: R4 es un éster monofosfato o trifosfato; o R4 es R7 es fenilo opcionalmente sustituido, naftilo opcionalmente sustituido, o indolilo opcionalmente sustituido; R8 y R8`are hidrógeno, alquilo C1-C6, bencilo, o fenilo; o R8 y R8` forman cicloalquilo C3-C7; R9 es alquilo C1-C10, cicloalquilo C3-C7, fenilo o fenil-alquilo C1-C6, en donde la porción fenilo en el fenilo o en el fenil-alquilo C1-C6 está opcionalmente sustituida; o una sal o un solvato farmacéuticamente aceptable de los mismos; formulaciones farmacéuticas y el uso de los compuestos I como inhibidotes del VHC.
UY0001032642A 2009-05-14 2010-05-14 Espironucleósidos uracílicos oxetánicos UY32642A (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP09160215 2009-05-14

Publications (1)

Publication Number Publication Date
UY32642A true UY32642A (es) 2010-11-30

Family

ID=40823307

Family Applications (1)

Application Number Title Priority Date Filing Date
UY0001032642A UY32642A (es) 2009-05-14 2010-05-14 Espironucleósidos uracílicos oxetánicos

Country Status (39)

Country Link
US (2) US8481510B2 (es)
EP (2) EP2511282B1 (es)
JP (2) JP5778135B2 (es)
KR (1) KR101806837B1 (es)
CN (1) CN102439024B (es)
AP (1) AP2783A (es)
AR (1) AR076579A1 (es)
AU (1) AU2010247439B2 (es)
BR (1) BRPI1010579A2 (es)
CA (1) CA2760329C (es)
CL (1) CL2011002859A1 (es)
CO (1) CO6440533A2 (es)
CR (1) CR20120297A (es)
CY (2) CY1114081T1 (es)
DK (2) DK2430035T3 (es)
EA (1) EA022084B1 (es)
EC (1) ECSP11011461A (es)
ES (2) ES2411086T3 (es)
HK (1) HK1166326A1 (es)
HN (1) HN2011003014A (es)
HR (2) HRP20130554T1 (es)
IL (1) IL215955A (es)
JO (1) JO3027B1 (es)
ME (1) ME01478B (es)
MX (1) MX2011012027A (es)
MY (1) MY157018A (es)
NI (1) NI201100197A (es)
NZ (1) NZ596073A (es)
PL (2) PL2511282T3 (es)
PT (2) PT2430035E (es)
RS (1) RS52822B (es)
SG (1) SG175981A1 (es)
SI (2) SI2511282T1 (es)
SM (2) SMT201300078B (es)
TW (1) TWI461432B (es)
UA (1) UA105790C2 (es)
UY (1) UY32642A (es)
WO (1) WO2010130726A1 (es)
ZA (1) ZA201108309B (es)

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US8173621B2 (en) 2008-06-11 2012-05-08 Gilead Pharmasset Llc Nucleoside cyclicphosphates
JP5793084B2 (ja) 2008-12-23 2015-10-14 ギリアド ファーマセット エルエルシー プリンヌクレオシドの合成
JO3027B1 (ar) 2009-05-14 2016-09-05 Janssen Products Lp نيوكليوسيدات يوراسيل سبيرواوكسيتان
ES2605433T3 (es) * 2010-11-10 2017-03-14 Janssen Products, L.P. Fosforamidatos de espironucleósido oxetánico uracílico
WO2012062870A1 (en) * 2010-11-10 2012-05-18 Janssen Products, Lp Uracyl spirooxetane nucleoside phosphoramidates
PT3042910T (pt) * 2010-11-30 2019-04-16 Gilead Pharmasset Llc 2'-espiro-nucleósidos para utilização na terapia da hepatite c
AU2015252113B2 (en) * 2010-11-30 2017-05-04 Gilead Pharmasset Llc Compounds
WO2012142523A2 (en) * 2011-04-13 2012-10-18 Gilead Sciences, Inc. 1'-substituted pyrimidine n-nucleoside analogs for antiviral treatment
CA2860234A1 (en) * 2011-12-22 2013-06-27 Alios Biopharma, Inc. Substituted phosphorothioate nucleotide analogs
EA027929B1 (ru) 2012-05-25 2017-09-29 Янссен Сайенсиз Айрлэнд Юси Нуклеозиды на основе урацила и спирооксетана
BR112015020472B1 (pt) * 2013-03-08 2021-01-19 Nanjing Sanhome Pharmaceutical Co., Ltd. composto de fosforamidato de nucleosídeo, composição farmacêutica e uso do mesmo
BR112015025716A2 (pt) 2013-04-12 2017-07-18 Achillion Pharmaceuticals Inc pró-fármacos de nucleosídeo submetidos a deutério úteis para o tratamento de hcv
WO2014194826A1 (zh) * 2013-06-06 2014-12-11 南京圣和药业有限公司 三环稠杂环类核苷氨基磷酸酯化合物、其制备方法及应用
US20170165287A1 (en) * 2013-11-28 2017-06-15 Janssen Sciences Ireland Uc Crystal form of a nucleoside inhibitor of hcv
UA124966C2 (uk) 2015-03-06 2021-12-22 Атеа Фармасеутікалс, Інк. <font face="Symbol">b</font>-D-2'-ДЕЗОКСИ-2'-<font face="Symbol">a</font>-ФТОР-2'-<font face="Symbol">b</font>-C-ЗАМІЩЕНІ-2-МОДИФІКОВАНІ-N<sup>6</sup>-ЗАМІЩЕНІ ПУРИНОВІ НУКЛЕОТИДИ ДЛЯ ЛІКУВАННЯ ВИКЛИКАНИХ HCV ЗАХВОРЮВАНЬ
LU100724B1 (en) 2016-07-14 2018-07-31 Atea Pharmaceuticals Inc Beta-d-2'-deoxy-2'-alpha-fluoro-2'-beta-c-substituted-4'-fluoro-n6-substituted-6-amino-2-substituted purine nucleotides for the treatment of hepatitis c virus infection
EP3865136A1 (en) 2016-09-07 2021-08-18 ATEA Pharmaceuticals, Inc. 2'-substituted-n6-substituted purine nucleotides for corona virus treatment
KR20230151050A (ko) 2017-02-01 2023-10-31 아테아 파마슈티컬즈, 인크. C형 간염 바이러스를 치료하기 위한 뉴클레오티드 헤미-술페이트 염
TW202012001A (zh) 2018-04-10 2020-04-01 美商亞堤製藥公司 C型肝炎病毒(hcv)感染硬化之患者的治療
US10874687B1 (en) 2020-02-27 2020-12-29 Atea Pharmaceuticals, Inc. Highly active compounds against COVID-19
CN115443138A (zh) * 2020-04-14 2022-12-06 杨森制药公司 用于治疗戊型肝炎的螺环核苷类似物

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WO2002057287A2 (en) * 2001-01-22 2002-07-25 Merck & Co., Inc. Nucleoside derivatives as inhibitors of rna-dependent rna viral polymerase
US20070265222A1 (en) * 2004-06-24 2007-11-15 Maccoss Malcolm Nucleoside Aryl Phosphoramidates for the Treatment of Rna-Dependent Rna Viral Infection
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PA8852101A1 (es) * 2008-12-08 2010-07-27 Medivir Ab Nucleótidos uracil ciclopropílicos
JO3027B1 (ar) * 2009-05-14 2016-09-05 Janssen Products Lp نيوكليوسيدات يوراسيل سبيرواوكسيتان

Also Published As

Publication number Publication date
PT2511282E (pt) 2014-07-11
CA2760329A1 (en) 2010-11-18
AU2010247439B2 (en) 2014-09-25
IL215955A0 (en) 2012-01-31
IL215955A (en) 2015-03-31
KR20120018355A (ko) 2012-03-02
EP2430035B1 (en) 2013-04-03
AU2010247439A1 (en) 2011-12-01
CN102439024B (zh) 2014-09-17
ECSP11011461A (es) 2012-02-29
SMT201300078B (it) 2013-09-06
PT2430035E (pt) 2013-05-22
TWI461432B (zh) 2014-11-21
HRP20140605T1 (hr) 2014-09-26
UA105790C2 (uk) 2014-06-25
NZ596073A (en) 2013-02-22
ME01478B (me) 2014-04-20
EA022084B1 (ru) 2015-10-30
CR20120297A (es) 2012-10-25
MX2011012027A (es) 2012-02-28
PL2430035T3 (pl) 2013-08-30
ZA201108309B (en) 2013-04-24
SMT201400085B (it) 2014-09-08
HRP20130554T1 (en) 2013-07-31
JP5778135B2 (ja) 2015-09-16
BRPI1010579A2 (pt) 2016-03-15
KR101806837B1 (ko) 2017-12-08
US20120065156A1 (en) 2012-03-15
AP2011005958A0 (en) 2011-10-31
SI2511282T1 (sl) 2014-09-30
DK2511282T3 (da) 2014-07-07
AP2783A (en) 2013-10-31
EA201171406A1 (ru) 2012-05-30
US20130217648A1 (en) 2013-08-22
CN102439024A (zh) 2012-05-02
AR076579A1 (es) 2011-06-22
HN2011003014A (es) 2014-06-30
JP2012526764A (ja) 2012-11-01
HK1166326A1 (en) 2012-10-26
US8481510B2 (en) 2013-07-09
TW201100442A (en) 2011-01-01
PL2511282T3 (pl) 2014-09-30
NI201100197A (es) 2012-05-28
US8933052B2 (en) 2015-01-13
EP2511282A1 (en) 2012-10-17
CL2011002859A1 (es) 2012-07-20
CY1115383T1 (el) 2017-01-04
DK2430035T3 (da) 2013-05-27
ES2411086T3 (es) 2013-07-04
EP2511282B1 (en) 2014-04-02
SI2430035T1 (sl) 2013-08-30
MY157018A (en) 2016-04-15
JO3027B1 (ar) 2016-09-05
WO2010130726A1 (en) 2010-11-18
CO6440533A2 (es) 2012-05-15
ES2477598T3 (es) 2014-07-17
SG175981A1 (en) 2011-12-29
EP2430035A1 (en) 2012-03-21
CY1114081T1 (el) 2016-07-27
JP2015180692A (ja) 2015-10-15
RS52822B (en) 2013-10-31
CA2760329C (en) 2017-10-31

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