WO1994003467A3 - Antiretroviral enantiomeric nucleotide analogs - Google Patents

Antiretroviral enantiomeric nucleotide analogs Download PDF

Info

Publication number
WO1994003467A3
WO1994003467A3 PCT/US1993/007360 US9307360W WO9403467A3 WO 1994003467 A3 WO1994003467 A3 WO 1994003467A3 US 9307360 W US9307360 W US 9307360W WO 9403467 A3 WO9403467 A3 WO 9403467A3
Authority
WO
WIPO (PCT)
Prior art keywords
antiretroviral
nucleotide analogs
enantiomeric nucleotide
enantiomeric
aza
Prior art date
Application number
PCT/US1993/007360
Other languages
French (fr)
Other versions
WO1994003467B1 (en
WO1994003467A2 (en
Inventor
Antonin Holy
Hana Dvorakova
Erik Desire Alice Declercq
Jan Marie Rene Balzarini
Original Assignee
Inst Organic Chem Biochem
Stichting Rega V Z W
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 Inst Organic Chem Biochem, Stichting Rega V Z W, Gilead Sciences Inc filed Critical Inst Organic Chem Biochem
Priority to JP1994505559A priority Critical patent/JP3561272B6/en
Priority to DK93918659T priority patent/DK0654037T3/en
Priority to DE69324923T priority patent/DE69324923T2/en
Priority to EP93918659A priority patent/EP0654037B1/en
Priority to CA002141589A priority patent/CA2141589C/en
Priority to US08/379,551 priority patent/US6653296B1/en
Publication of WO1994003467A2 publication Critical patent/WO1994003467A2/en
Publication of WO1994003467A3 publication Critical patent/WO1994003467A3/en
Publication of WO1994003467B1 publication Critical patent/WO1994003467B1/en
Priority to HK98113194A priority patent/HK1011998A1/en
Priority to GR990401839T priority patent/GR3030754T3/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/47—One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/04—Immunostimulants
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
    • C07D309/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D309/08—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D309/10—Oxygen atoms
    • C07D309/12—Oxygen atoms only hydrogen atoms and one oxygen atom directly attached to ring carbon atoms, e.g. tetrahydropyranyl ethers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
    • C07D473/16—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
    • C07D473/18—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 one oxygen and one nitrogen atom, e.g. guanine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/32—Nitrogen atom
    • C07D473/34—Nitrogen atom attached in position 6, e.g. adenine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/28—Phosphorus compounds with one or more P—C bonds
    • C07F9/38—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
    • C07F9/40—Esters thereof
    • C07F9/4003—Esters thereof the acid moiety containing a substituent or a structure which is considered as characteristic
    • C07F9/4006—Esters of acyclic acids which can have further substituents on alkyl
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/645—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having two nitrogen atoms as the only ring hetero atoms
    • C07F9/6509—Six-membered rings
    • C07F9/6512—Six-membered rings having the nitrogen atoms in positions 1 and 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6515—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having three nitrogen atoms as the only ring hetero atoms
    • C07F9/6521—Six-membered rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
    • C07F9/65616—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings containing the ring system having three or more than three double bonds between ring members or between ring members and non-ring members, e.g. purine or analogs

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Virology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Immunology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pyrane Compounds (AREA)
  • Micro-Organisms Or Cultivation Processes Thereof (AREA)

Abstract

Resolved enantiomers of formulae (IA) and (IB) wherein B is a purine or pyrimidine base or aza and/or deaza analogs thereof are useful in antiviral pharmaceutical compositions to treat retroviral infections.
PCT/US1993/007360 1992-08-05 1993-08-04 Antiretroviral enantiomeric nucleotide analogs WO1994003467A2 (en)

Priority Applications (8)

Application Number Priority Date Filing Date Title
JP1994505559A JP3561272B6 (en) 1992-08-05 1993-08-04 Antiretroviral enantiomeric nucleotide analogues
DK93918659T DK0654037T3 (en) 1992-08-05 1993-08-04 Enantiomeric anti-retroviral nucleotide analogues
DE69324923T DE69324923T2 (en) 1992-08-05 1993-08-04 Antiretroviral, enantiomeric nucleotide analogs
EP93918659A EP0654037B1 (en) 1992-08-05 1993-08-04 Antiretroviral enantiomeric nucleotide analogs
CA002141589A CA2141589C (en) 1992-08-05 1993-08-04 Antiretroviral enantiomeric nucleotide analogs
US08/379,551 US6653296B1 (en) 1992-08-05 1993-08-04 Antiretroviral enantiomeric nucleotide analogs
HK98113194A HK1011998A1 (en) 1992-08-05 1998-12-11 Antiretroviral enantiomeric nucleotide analogs
GR990401839T GR3030754T3 (en) 1992-08-05 1999-07-14 Antiretroviral enantiomeric nucleotide analogs.

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US07/925,610 1992-08-05
US07/925,610 US6057305A (en) 1992-08-05 1992-08-05 Antiretroviral enantiomeric nucleotide analogs

Publications (3)

Publication Number Publication Date
WO1994003467A2 WO1994003467A2 (en) 1994-02-17
WO1994003467A3 true WO1994003467A3 (en) 1994-06-23
WO1994003467B1 WO1994003467B1 (en) 1994-07-21

Family

ID=25451994

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US1993/007360 WO1994003467A2 (en) 1992-08-05 1993-08-04 Antiretroviral enantiomeric nucleotide analogs

Country Status (13)

Country Link
US (3) US6057305A (en)
EP (2) EP0654037B1 (en)
JP (2) JP4083691B2 (en)
AT (1) ATE179983T1 (en)
CA (2) CA2141589C (en)
CZ (2) CZ290797B6 (en)
DE (1) DE69324923T2 (en)
DK (1) DK0654037T3 (en)
ES (1) ES2131116T3 (en)
GR (1) GR3030754T3 (en)
HK (1) HK1011998A1 (en)
SG (1) SG47761A1 (en)
WO (1) WO1994003467A2 (en)

Families Citing this family (95)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6057305A (en) * 1992-08-05 2000-05-02 Institute Of Organic Chemistry And Biochemistry Of The Academy Of Sciences Of The Czech Republic Antiretroviral enantiomeric nucleotide analogs
US5798340A (en) * 1993-09-17 1998-08-25 Gilead Sciences, Inc. Nucleotide analogs
KR100386685B1 (en) * 1993-09-17 2003-12-31 길리애드 사이언시즈, 인코포레이티드 Nucleotide Homolog
IT1270008B (en) * 1994-09-23 1997-04-16 Ist Superiore Sanita PURINIC AND 8-AZAPURINIC DERIVATIVES FOR THE THERAPEUTIC TREATMENT OF AIDS
US5977061A (en) * 1995-04-21 1999-11-02 Institute Of Organic Chemistry And Biochemistry Of The Academy Of Sciences Of The Czech Republic N6 - substituted nucleotide analagues and their use
KR19990022752A (en) * 1995-06-15 1999-03-25 미우라 아끼라 Phosphonate nucleotide derivatives
US6093816A (en) 1996-06-27 2000-07-25 Isis Pharmaceuticals, Inc. Cationic lipids
DK0915894T3 (en) * 1996-07-26 2003-09-15 Gilead Sciences Inc nucleotide analogs
US5922695A (en) * 1996-07-26 1999-07-13 Gilead Sciences, Inc. Antiviral phosphonomethyoxy nucleotide analogs having increased oral bioavarilability
US5733788A (en) * 1996-07-26 1998-03-31 Gilead Sciences, Inc. PMPA preparation
EP1243593B1 (en) * 1997-07-25 2005-09-21 Gilead Sciences, Inc. Nucleotide analog composition and synthesis method
US5935946A (en) * 1997-07-25 1999-08-10 Gilead Sciences, Inc. Nucleotide analog composition and synthesis method
ATE288914T1 (en) * 1997-07-25 2005-02-15 Gilead Sciences Inc NUCLEOTIDE ANALOG COMPOSITION AND SYNTHESIS METHOD
DE69840216D1 (en) 1997-08-08 2008-12-24 Celmed Oncology Usa Inc Methods and preparations for overcoming resistance to biological or chemical therapies
US7462605B2 (en) * 1998-01-23 2008-12-09 Celmed Oncology (Usa), Inc. Phosphoramidate compounds and methods of use
PT1045897E (en) 1998-01-23 2002-07-31 Newbiotics Inc THERAPEUTIC AGENTS BY ENZYMATIC CATALOG
US6683061B1 (en) 1999-07-22 2004-01-27 Newbiotics, Inc. Enzyme catalyzed therapeutic activation
EP1200130A2 (en) 1999-07-22 2002-05-02 Newbiotics, Inc. Methods for treating therapy-resistant tumors
WO2001044257A1 (en) * 1999-12-17 2001-06-21 Ariad Pharmaceuticals, Inc. Proton pump inhibitors
CN1291994C (en) 2000-07-21 2006-12-27 吉里德科学公司 Prodrugs of phosphonate nucleotide analogues and methods for selecting and making same
CA2441350A1 (en) 2001-01-19 2002-07-25 Newbiotics, Inc. Methods to treat autoimmune and inflammatory conditions
CA2452036C (en) 2001-06-29 2009-09-29 Institute Of Organic Chemistry And Biochemistry Of The Academy Of Sciences Of The Czech Republic 6-'2-(phosphonomethoxy) alkoxy pyrimidine derivatives having antiviral activity
JP2005508924A (en) * 2001-08-30 2005-04-07 三菱ウェルファーマ株式会社 Antiviral agent
US7388002B2 (en) * 2001-11-14 2008-06-17 Biocryst Pharmaceuticals, Inc. Nucleosides, preparation thereof and use as inhibitors of RNA viral polymerases
WO2003087298A2 (en) * 2001-11-14 2003-10-23 Biocryst Pharmaceuticals, Inc. Nucleosides preparation thereof and use as inhibitors of rna viral polymerases
IL163666A0 (en) 2002-02-22 2005-12-18 New River Pharmaceuticals Inc Active agent delivery systems and methods for protecting and administering active agents
KR20090053867A (en) 2003-01-14 2009-05-27 길리애드 사이언시즈, 인코포레이티드 Compositions and methods for combination antiviral therapy
EA011948B1 (en) 2003-06-16 2009-06-30 Инститьют Оф Оргэник Кемистри Энд Байокемистри, Экэдеми Оф Сайэнс Оф Зе Чек Рипаблик Phosphonate-substituted pyrimidine compounds (variants), method for preparation thereof (variants), pharmaceutical composition based thereon and method for the treatment of viral infection
WO2005090370A1 (en) * 2004-02-05 2005-09-29 The Regents Of The University Of California Pharmacologically active agents containing esterified phosphonates and methods for use thereof
UA93354C2 (en) 2004-07-09 2011-02-10 Гилиад Сайенсиз, Инк. Topical antiviral formulations
WO2006068760A2 (en) * 2004-11-19 2006-06-29 The Regents Of The University Of California Anti-inflammatory pyrazolopyrimidines
EP1831235B1 (en) 2004-12-16 2013-02-20 The Regents of The University of California Lung-targeted drugs
WO2006130217A2 (en) * 2005-04-01 2006-12-07 The Regents Of The University Of California Substituted phosphate esters of nucleoside phosphonates
AU2006239677A1 (en) * 2005-04-25 2006-11-02 Institute Of Organic Chemistry And Biochemistry Of The Academy Of Sciences Of The Czech Republic Use of compounds to enhance processivity of telomerase
TWI471145B (en) 2005-06-13 2015-02-01 Bristol Myers Squibb & Gilead Sciences Llc Unitary pharmaceutical dosage form
TWI375560B (en) 2005-06-13 2012-11-01 Gilead Sciences Inc Composition comprising dry granulated emtricitabine and tenofovir df and method for making the same
AP2008004533A0 (en) * 2005-12-14 2008-08-31 Cipla Ltd Pharmaceutical combination
PT2004654E (en) * 2006-04-04 2013-08-27 Univ California Pyrazolopyrimidine derivatives for use as kinase antagonists
US7951789B2 (en) 2006-12-28 2011-05-31 Idenix Pharmaceuticals, Inc. Compounds and pharmaceutical compositions for the treatment of viral infections
US20080318904A1 (en) * 2007-06-20 2008-12-25 Protia, Llc Deuterium-enriched tenofovir
US20110160232A1 (en) * 2007-10-04 2011-06-30 Pingda Ren Certain chemical entities and therapeutic uses thereof
JP5869222B2 (en) 2008-01-04 2016-02-24 インテリカイン， エルエルシー Specific chemical entities, compositions and methods
US8193182B2 (en) 2008-01-04 2012-06-05 Intellikine, Inc. Substituted isoquinolin-1(2H)-ones, and methods of use thereof
TWI444384B (en) 2008-02-20 2014-07-11 Gilead Sciences Inc Nucleotide analogues and their use in the treatment of malignancies
US8637542B2 (en) * 2008-03-14 2014-01-28 Intellikine, Inc. Kinase inhibitors and methods of use
US8993580B2 (en) 2008-03-14 2015-03-31 Intellikine Llc Benzothiazole kinase inhibitors and methods of use
RU2519947C2 (en) * 2008-07-02 2014-06-20 Айденикс Фармасьютикалз, Инк. Compounds and pharmaceutical compositions for treatment of viral diseases
MX2011000216A (en) * 2008-07-08 2011-03-29 Intellikine Inc Kinase inhibitors and methods of use.
US20110224223A1 (en) 2008-07-08 2011-09-15 The Regents Of The University Of California, A California Corporation MTOR Modulators and Uses Thereof
CA2738429C (en) 2008-09-26 2016-10-25 Intellikine, Inc. Heterocyclic kinase inhibitors
WO2010045542A2 (en) 2008-10-16 2010-04-22 The Regents Of The University Of California Fused ring heteroaryl kinase inhibitors
US8476282B2 (en) * 2008-11-03 2013-07-02 Intellikine Llc Benzoxazole kinase inhibitors and methods of use
CA2760791C (en) 2009-05-07 2017-06-20 Intellikine, Inc. Heterocyclic compounds and uses thereof
US8980899B2 (en) 2009-10-16 2015-03-17 The Regents Of The University Of California Methods of inhibiting Ire1
CN102917585A (en) 2010-04-01 2013-02-06 埃迪尼克斯医药公司 Compounds and pharmaceutical compositions for the treatment of viral infections
AU2011255218B2 (en) 2010-05-21 2015-03-12 Infinity Pharmaceuticals, Inc. Chemical compounds, compositions and methods for kinase modulation
EP2579892A2 (en) 2010-06-09 2013-04-17 Vaccine Technologies, Incorporated Therapeutic immunization in hiv infected subjects receiving stable antiretroviral treatment
NZ604037A (en) 2010-06-11 2014-11-28 Gilead Sciences Inc Topical antiviral formulations for prevention of transmission of hsv-2
JP2013545749A (en) 2010-11-10 2013-12-26 インフィニティー ファーマシューティカルズ， インコーポレイテッド Heterocyclic compounds and uses thereof
MX2013006127A (en) 2010-12-10 2013-09-26 Sigmapharm Lab Llc Highly stable compositions of orally active nucleotide analogues or orally active nucleotide analogue prodrugs.
ZA201103820B (en) 2010-12-13 2012-01-25 Laurus Labs Private Ltd Process for the preparation of tenofovir
CA2824197C (en) 2011-01-10 2020-02-25 Michael Martin Processes for preparing isoquinolinones and solid forms of isoquinolinones
JP6130305B2 (en) 2011-02-23 2017-05-17 インテリカイン， エルエルシー Combinations of kinase inhibitors and their use
CA2843324A1 (en) 2011-03-31 2012-11-15 Idenix Pharmaceuticals, Inc. Compounds and pharmaceutical compositions for the treatment of viral infections
US9650346B2 (en) 2011-04-08 2017-05-16 Laurus Labs Private Ltd. Solid forms of antiretroviral compounds, process for the preparation and their pharmaceutical composition thereof
CA2835321A1 (en) * 2011-05-10 2012-11-15 Okapi Sciences Nv Compounds for use in the treatment of feline retroviral infections
CN103930422A (en) 2011-07-19 2014-07-16 无限药品股份有限公司 Heterocyclic compounds and uses thereof
CA2842190A1 (en) 2011-07-19 2013-01-24 Infinity Pharmaceuticals Inc. Heterocyclic compounds and uses thereof
AR091790A1 (en) 2011-08-29 2015-03-04 Infinity Pharmaceuticals Inc DERIVATIVES OF ISOQUINOLIN-1-ONA AND ITS USES
JP6342805B2 (en) 2011-09-02 2018-06-13 ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア Substituted pyrazolo [3,4-D] pyrimidine and uses thereof
ES2627348T3 (en) 2011-11-16 2017-07-27 Laurus Labs Private Limited Tenofovir preparation process
CA2857490C (en) 2011-12-22 2020-03-31 Geron Corporation Guanine analogs as telomerase substrates and telomere length affectors
US8940742B2 (en) 2012-04-10 2015-01-27 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
US8828998B2 (en) 2012-06-25 2014-09-09 Infinity Pharmaceuticals, Inc. Treatment of lupus, fibrotic conditions, and inflammatory myopathies and other disorders using PI3 kinase inhibitors
CN103665043B (en) 2012-08-30 2017-11-10 江苏豪森药业集团有限公司 A kind of tenofovir prodrug and its application in medicine
CA2886240A1 (en) 2012-09-26 2014-04-03 The Regents Of The University Of California Modulation of ire1
EP3401320B1 (en) 2013-03-15 2020-05-13 The Regents of the University of California Acyclic nucleoside phosphonate diesters for use in treating human papilloma virus, cervical intraepithelial neoplasia, anal intraepithelial neoplasia, or vulvar intraepithelial neoplasia
US9481667B2 (en) 2013-03-15 2016-11-01 Infinity Pharmaceuticals, Inc. Salts and solid forms of isoquinolinones and composition comprising and methods of using the same
CN104230934B (en) * 2013-06-08 2016-12-28 上海医药工业研究院 A kind of compound and its production and use
MX2016004340A (en) 2013-10-04 2016-08-08 Infinity Pharmaceuticals Inc Heterocyclic compounds and uses thereof.
WO2015051241A1 (en) 2013-10-04 2015-04-09 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
CN103641857B (en) * 2013-12-20 2016-08-24 石药集团中诺药业（石家庄）有限公司 A kind of Novel tenofovir crystal form and preparation method thereof
TWI660965B (en) 2014-01-15 2019-06-01 美商基利科學股份有限公司 Solid forms of tenofovir
PT3119397T (en) 2014-03-19 2022-04-11 Infinity Pharmaceuticals Inc Heterocyclic compounds for use in the treatment of pi3k-gamma mediated disorders
WO2015160975A2 (en) 2014-04-16 2015-10-22 Infinity Pharmaceuticals, Inc. Combination therapies
RS63250B1 (en) 2014-09-15 2022-06-30 Univ California Nucleotide analogs
US9708348B2 (en) 2014-10-03 2017-07-18 Infinity Pharmaceuticals, Inc. Trisubstituted bicyclic heterocyclic compounds with kinase activities and uses thereof
RS62434B1 (en) 2014-12-26 2021-11-30 Univ Emory Anti-viral n4-hydroxycytidine derivatives
US10160761B2 (en) 2015-09-14 2018-12-25 Infinity Pharmaceuticals, Inc. Solid forms of isoquinolinones, and process of making, composition comprising, and methods of using the same
US10377782B2 (en) 2015-09-15 2019-08-13 The Regents Of The University Of California Nucleotide analogs
WO2017161116A1 (en) 2016-03-17 2017-09-21 Infinity Pharmaceuticals, Inc. Isotopologues of isoquinolinone and quinazolinone compounds and uses thereof as pi3k kinase inhibitors
US10919914B2 (en) 2016-06-08 2021-02-16 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
MX2018016227A (en) 2016-06-24 2019-07-08 Infinity Pharmaceuticals Inc Combination therapies.
KR102626210B1 (en) 2017-12-07 2024-01-18 에모리 유니버시티 N4-hydroxycytidine and derivatives and anti-viral uses related thereto
WO2021209563A1 (en) 2020-04-16 2021-10-21 Som Innovation Biotech, S.A. Compounds for use in the treatment of viral infections by respiratory syndrome-related coronavirus

Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1544419A (en) * 1975-11-19 1979-04-19 Science Union & Cie Purines and pyrazolo-pyrimidines a process for their preparation and pharmaceutical compositions containing them
EP0009155A1 (en) * 1978-09-15 1980-04-02 Newport Pharmaceuticals International, Inc. 9-Hydroxyalkyl-purines, processes for preparing them and therapeutical composition containing the 9-hydroxyalkyl-purines as active ingredients
EP0130126A1 (en) * 1983-06-24 1985-01-02 Merck & Co. Inc. (S)-9-(2,3-dihydroxy-1-propoxymethyl) guanine and its acyl derivatives, their preparation and their application as antiherpetic agents
EP0253412A2 (en) * 1986-07-18 1988-01-20 Ceskoslovenska akademie ved N-Phosphonylmethoxyalkyl derivatives of pyrimidine and purine bases, methods for their preparation and pharmaceutical compositions therefrom with antiviral activity
EP0292244A2 (en) * 1987-05-18 1988-11-23 Canon Kabushiki Kaisha Polymeric liquid crystal composition and liquid crystal device
EP0322815A2 (en) * 1987-12-25 1989-07-05 Daiichi Pharmaceutical Co., Ltd. Propoxybenzene derivatives and process for preparing the same
EP0368410A2 (en) * 1988-11-07 1990-05-16 Gist-Brocades N.V. Optically active benzoxazines and bezothiazines and a process for their stereospecific preparation
DE3906357A1 (en) * 1989-03-01 1990-09-06 Boehringer Mannheim Gmbh NEW ACYCLIC NUCLEOSIDE ANALOG, METHOD FOR THE PRODUCTION AND USE OF THESE COMPOUNDS AS ANTIVIRAL MEDICINAL PRODUCTS
EP0452935A1 (en) * 1990-04-20 1991-10-23 Institute Of Organic Chemistry And Biochemistry Of The Academy Of Sciences Of The Czech Republic Chiral 2-(phosphonomethoxy)propyl guanines as antiviral agents

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB544419A (en) * 1940-01-08 1942-04-13 Union Special Machine Co Improvements in or relating to sewing machines
CS233665B1 (en) * 1983-01-06 1985-03-14 Antonin Holy Processing of isomere o-phosphonylmethylderivative of anantiomere racemic vicinal diene
US4556727A (en) * 1984-07-18 1985-12-03 University Patents, Inc. Ferroelectric smectic liquid crystals
CS263951B1 (en) * 1985-04-25 1989-05-12 Antonin Holy 9-(phosponylmethoxyalkyl)adenines and method of their preparation
CS263952B1 (en) * 1985-04-25 1989-05-12 Holy Antonin Remedy with antiviral effect
EP0264106B1 (en) * 1986-10-14 1994-03-16 Banyu Pharmaceutical Co., Ltd. 5-Substituted amino-4-hydroxy-pentanoic acid derivatives and their use
NZ222553A (en) * 1986-11-18 1991-07-26 Bristol Myers Co Phosphonomethoxyalkylene purine and pyrimidine derivatives and pharmaceutical compositions
US5650510A (en) * 1986-11-18 1997-07-22 Institute Of Organic Chemistry And Biochemistry Of The Academy Of Sciences Of The Czech Republic Antiviral phosphonomethoxyalkylene purine and pyrimidine derivatives
JP2580205B2 (en) * 1987-10-21 1997-02-12 チッソ株式会社 Optically active-2-biphenylylpyridines
US5466806A (en) * 1989-02-08 1995-11-14 Biochem Pharma Inc. Processes for preparing substituted 1,3-oxathiolanes with antiviral properties
US5302585A (en) * 1990-04-20 1994-04-12 Institute Of Organic Chemistry And Biochemistry Of The Academy Of Sciences Of The Czech Republic Use of chiral 2-(phosphonomethoxy)propyl guanines as antiviral agents
SK280313B6 (en) * 1990-04-24 1999-11-08 �Stav Organick� Chemie A Biochemie Av �R N-(3-fluoro-2-phosphonylmethoxypropyl) derivatives of purine and pyrimidine heterocyclic bases, process for their preparation and their use
CS276072B6 (en) * 1990-08-06 1992-03-18 Ustav Organicke Chemie A Bioch (2R)-2-/DI(2-PROPYL)PHOSPHONYLMETHOXY/-3-p-TOLUENESULFONYLOXY -1- TRIMETHYLACETOXYPROPANE AND PROCESS FOR PREPARING THEREOF
KR100221981B1 (en) * 1990-08-10 1999-09-15 안토닌 포레이트 Novel process for the preparation of nucleotides
EP0481214B1 (en) * 1990-09-14 1998-06-24 Institute Of Organic Chemistry And Biochemistry Of The Academy Of Sciences Of The Czech Republic Prodrugs of phosphonates
US6057305A (en) * 1992-08-05 2000-05-02 Institute Of Organic Chemistry And Biochemistry Of The Academy Of Sciences Of The Czech Republic Antiretroviral enantiomeric nucleotide analogs
EP0763048A1 (en) * 1994-05-31 1997-03-19 Medivir Aktiebolag Post exposure prevention of hiv

Patent Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1544419A (en) * 1975-11-19 1979-04-19 Science Union & Cie Purines and pyrazolo-pyrimidines a process for their preparation and pharmaceutical compositions containing them
EP0009155A1 (en) * 1978-09-15 1980-04-02 Newport Pharmaceuticals International, Inc. 9-Hydroxyalkyl-purines, processes for preparing them and therapeutical composition containing the 9-hydroxyalkyl-purines as active ingredients
EP0130126A1 (en) * 1983-06-24 1985-01-02 Merck & Co. Inc. (S)-9-(2,3-dihydroxy-1-propoxymethyl) guanine and its acyl derivatives, their preparation and their application as antiherpetic agents
EP0253412A2 (en) * 1986-07-18 1988-01-20 Ceskoslovenska akademie ved N-Phosphonylmethoxyalkyl derivatives of pyrimidine and purine bases, methods for their preparation and pharmaceutical compositions therefrom with antiviral activity
EP0292244A2 (en) * 1987-05-18 1988-11-23 Canon Kabushiki Kaisha Polymeric liquid crystal composition and liquid crystal device
EP0322815A2 (en) * 1987-12-25 1989-07-05 Daiichi Pharmaceutical Co., Ltd. Propoxybenzene derivatives and process for preparing the same
EP0368410A2 (en) * 1988-11-07 1990-05-16 Gist-Brocades N.V. Optically active benzoxazines and bezothiazines and a process for their stereospecific preparation
DE3906357A1 (en) * 1989-03-01 1990-09-06 Boehringer Mannheim Gmbh NEW ACYCLIC NUCLEOSIDE ANALOG, METHOD FOR THE PRODUCTION AND USE OF THESE COMPOUNDS AS ANTIVIRAL MEDICINAL PRODUCTS
EP0452935A1 (en) * 1990-04-20 1991-10-23 Institute Of Organic Chemistry And Biochemistry Of The Academy Of Sciences Of The Czech Republic Chiral 2-(phosphonomethoxy)propyl guanines as antiviral agents

Non-Patent Citations (5)

* Cited by examiner, † Cited by third party
Title
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY vol. no. 2 , 1993, pages 332-8 J.BALZARINI ' Differential Antiherpesvirus and Anti- virus Effects ' *
ANTIVIRAL CHEMISTRY & CHEMOTHERAPY vol.2 no. 6, 1991, pages 329-336 P. CLAYETTE ' Anti-HIV activities of novel nucleoside analogues ' *
EUR. J. MED. CHEM.-- CHIM. THER. vol. 17, (1982) pages 569-576 L. COLLA ' Synthesis of aliphatic nucleoside analog with potential antiviral activity ' *
FUMIO SUGAWARA: "Stereoselective Synthesis of 1- and 2-O-alpha-D-Cellotriosyl-3-deoxy-2(R)- and 2(S)-glycerols Related to Rhynchosporoside", AGRICULTURAL AND BIOLOGICAL CHEMISTRY, vol. 50, no. 9, 1986, TOKYO JP, pages 2261 - 2271 *
HOWARD J. SCHAEFFER: "Enzyme Inhibitors. VIII. Studies on the Mode of Binding of Some 6-Substituted 9-(Hydroxyalkyl)purines to Adenosine Deaminase", JOURNAL OF MEDICINAL CHEMISTRY, vol. 8, no. 4, 1965, WASHINGTON US, pages 502 - 506 *

Also Published As

Publication number Publication date
US6057305A (en) 2000-05-02
DK0654037T3 (en) 1999-11-01
US6479673B1 (en) 2002-11-12
SG47761A1 (en) 1998-04-17
DE69324923D1 (en) 1999-06-17
EP0654037B1 (en) 1999-05-12
ES2131116T3 (en) 1999-07-16
CA2141589A1 (en) 1994-02-17
EP0654037A1 (en) 1995-05-24
DE69324923T2 (en) 1999-11-25
JP2004189750A (en) 2004-07-08
JPH08503927A (en) 1996-04-30
CZ293533B6 (en) 2004-05-12
US6653296B1 (en) 2003-11-25
CA2574904A1 (en) 1994-02-17
ATE179983T1 (en) 1999-05-15
JP4083691B2 (en) 2008-04-30
CA2141589C (en) 2007-04-17
CZ290797B6 (en) 2002-10-16
JP3561272B2 (en) 2004-09-02
CA2574904C (en) 2009-06-16
JP2008120820A (en) 2008-05-29
CZ27295A3 (en) 1995-12-13
WO1994003467A2 (en) 1994-02-17
EP0897917A1 (en) 1999-02-24
HK1011998A1 (en) 1999-07-23
GR3030754T3 (en) 1999-11-30

Similar Documents

Publication Publication Date Title
WO1994003467A3 (en) Antiretroviral enantiomeric nucleotide analogs
IL84810A (en) Pharmaceutical antiviral compositions containing 1-beta-d-arabinofuranosyl-5-(1-alkynyl)cytosine and uracil derivatives thereof,some new such compounds and their preparation
AU4690989A (en) Antiviral cytosine and guanine derivatives
CA2479846A1 (en) Phosphonomethoxymethylpurine/pyrimidine derivatives
ATE159027T1 (en) NUCLEOSIDES CONTAINING BORON
EP0222330A3 (en) N6-substituted-5'-oxidized adenosine analogs
MY103801A (en) Dideoxydidehydrocarbocyclic nucleosides
ATE124412T1 (en) ANTIVIRUS DERIVATIVES OF (PHOSPHONEMETHOXY)METHOXY PURINE/PYRIMIDINE.
GB9205071D0 (en) Therapeutic nucleosides
ES8706163A1 (en) Nucleoside derivatives
ES2105684T3 (en) UNSATURATED DERIVATIVES OF PURINE AND PIRIMIDINE PHOSPHONATE.
AU6005586A (en) Antiviral compounds
PT85582A (en) Process for the preparation of novel 9-deazaguanines and of pharmaceutical compositions containing them
AU2476388A (en) Therapeutic necleosides
EP0219838A3 (en) Carbocyclic purine nucleosides, their production and use
EP0335770A3 (en) Novel fluorophosphonate nucleotide derivatives
EP0306597A3 (en) Antiviral nucleosides
JPS6422853A (en) Nucleoside analog
AU4544289A (en) Antiviral 5-propynyl pyrimidine nucleosides
GB9506644D0 (en) Preparation of nucleoside analogues
ECSP993155A (en) CHEMICAL COMPOUNDS

Legal Events

Date Code Title Description
AK Designated states

Kind code of ref document: A2

Designated state(s): CA CZ JP US

AL Designated countries for regional patents

Kind code of ref document: A2

Designated state(s): AT BE CH DE DK ES FR GB GR IE IT LU MC NL PT SE

121 Ep: the epo has been informed by wipo that ep was designated in this application
DFPE Request for preliminary examination filed prior to expiration of 19th month from priority date (pct application filed before 20040101)
AK Designated states

Kind code of ref document: A3

Designated state(s): CA CZ JP US

AL Designated countries for regional patents

Kind code of ref document: A3

Designated state(s): AT BE CH DE DK ES FR GB GR IE IT LU MC NL PT SE

WWE Wipo information: entry into national phase

Ref document number: 2141589

Country of ref document: CA

WWE Wipo information: entry into national phase

Ref document number: 08379551

Country of ref document: US

WWE Wipo information: entry into national phase

Ref document number: PV1995-272

Country of ref document: CZ

WWE Wipo information: entry into national phase

Ref document number: 1993918659

Country of ref document: EP

WWP Wipo information: published in national office

Ref document number: 1993918659

Country of ref document: EP

WWP Wipo information: published in national office

Ref document number: PV2001-529

Country of ref document: CZ

Ref document number: PV1995-272

Country of ref document: CZ

WWG Wipo information: grant in national office

Ref document number: 1993918659

Country of ref document: EP

WWE Wipo information: entry into national phase

Ref document number: PV2001-529

Country of ref document: CZ

WWG Wipo information: grant in national office

Ref document number: PV1995-272

Country of ref document: CZ

WWG Wipo information: grant in national office

Ref document number: PV2001-529

Country of ref document: CZ