DE69314239D1 - Verfahren zur Stereoselektivglycosylierung - Google Patents

Verfahren zur Stereoselektivglycosylierung

Info

Publication number
DE69314239D1
DE69314239D1 DE69314239T DE69314239T DE69314239D1 DE 69314239 D1 DE69314239 D1 DE 69314239D1 DE 69314239 T DE69314239 T DE 69314239T DE 69314239 T DE69314239 T DE 69314239T DE 69314239 D1 DE69314239 D1 DE 69314239D1
Authority
DE
Germany
Prior art keywords
stereoselective glycosylation
glycosylation method
stereoselective
anomer
fluorocarbohydrate
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Lifetime
Application number
DE69314239T
Other languages
English (en)
Other versions
DE69314239T2 (de
DE69314239C5 (de
Inventor
Ta-Sen Chou
Laurie Michelle Poteet
Douglas Patton Kjell
Cora Sue Grossman
Larry Wayne Hertel
Richard Elmer Holmes
Charles David Jones
Thomas Edward Mabry
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.)
Eli Lilly and Co
Original Assignee
Eli Lilly and Co
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=27583678&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=DE69314239(D1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Priority claimed from US07/902,312 external-priority patent/US5371210A/en
Priority claimed from US08/044,345 external-priority patent/US5594124A/en
Priority claimed from US08/044,343 external-priority patent/US5401838A/en
Priority claimed from US08/044,312 external-priority patent/US5426183A/en
Priority claimed from US08/044,996 external-priority patent/US5821357A/en
Application filed by Eli Lilly and Co filed Critical Eli Lilly and Co
Publication of DE69314239D1 publication Critical patent/DE69314239D1/de
Publication of DE69314239T2 publication Critical patent/DE69314239T2/de
Publication of DE69314239C5 publication Critical patent/DE69314239C5/de
Application granted granted Critical
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H17/00—Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
    • C07H17/04—Heterocyclic radicals containing only oxygen as ring hetero atoms
    • 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
DE69314239T 1992-06-22 1993-06-21 Verfahren zur Stereoselektivglycosylierung Expired - Lifetime DE69314239C5 (de)

Applications Claiming Priority (25)

Application Number Priority Date Filing Date Title
US902313 1986-08-28
US90213592A 1992-06-22 1992-06-22
US90215092A 1992-06-22 1992-06-22
US90231392A 1992-06-22 1992-06-22
US90230292A 1992-06-22 1992-06-22
US90211292A 1992-06-22 1992-06-22
US902302 1992-06-22
US902150 1992-06-22
US902135 1992-06-22
US902112 1992-06-22
US902312 1992-06-22
US07/902,312 US5371210A (en) 1992-06-22 1992-06-22 Stereoselective fusion glycosylation process for preparing 2'-deoxy-2',2'-difluoronucleosides and 2'-deoxy-2'-fluoronucleosides
US4431593A 1993-04-07 1993-04-07
US4430993A 1993-04-07 1993-04-07
US44996 1993-04-07
US44343 1993-04-07
US08/044,343 US5401838A (en) 1992-06-22 1993-04-07 Stereoselective fusion glycosylation process for preparing 2'-deoxy-2',2'-difluoronucleosides and 2'-deoxy-2'-fluoronucleosides
US44312 1993-04-07
US08/044,312 US5426183A (en) 1992-06-22 1993-04-07 Catalytic stereoselective glycosylation process for preparing 2'-deoxy-2',2'-difluoronucleosides and 2'-deoxy-2'-fluoronucleosides
US44345 1993-04-07
US08/044,996 US5821357A (en) 1992-06-22 1993-04-07 Stereoselective glycosylation process for preparing 2'-deoxy-2',2'-difluoropurine and triazole nucleosides
US44309 1993-04-07
US08/044,345 US5594124A (en) 1992-06-22 1993-04-07 Stereoselective glycosylation process for preparing 2'-Deoxy-2',2'-difluoropyrimidine nucleosides and 2'-deoxy-2'-fluoropyrimidine nucleosides and intermediates thereof
US44315 1993-04-07
EP93304817A EP0577303B1 (de) 1992-06-22 1993-06-21 Verfahren zur Stereoselektivglycosylierung

Publications (3)

Publication Number Publication Date
DE69314239D1 true DE69314239D1 (de) 1997-11-06
DE69314239T2 DE69314239T2 (de) 1998-02-19
DE69314239C5 DE69314239C5 (de) 2012-11-29

Family

ID=27583678

Family Applications (1)

Application Number Title Priority Date Filing Date
DE69314239T Expired - Lifetime DE69314239C5 (de) 1992-06-22 1993-06-21 Verfahren zur Stereoselektivglycosylierung

Country Status (20)

Country Link
EP (1) EP0577303B1 (de)
JP (1) JP3313191B2 (de)
KR (1) KR100252452B1 (de)
AT (1) ATE158799T1 (de)
BR (1) BR9302434A (de)
CA (1) CA2098881C (de)
CY (1) CY2067A (de)
DE (1) DE69314239C5 (de)
DK (1) DK0577303T3 (de)
ES (1) ES2107624T3 (de)
FI (1) FI108643B (de)
GR (1) GR3025689T3 (de)
HU (2) HUT64358A (de)
IL (1) IL106071A (de)
MX (1) MX9303707A (de)
MY (1) MY115775A (de)
NO (1) NO180235B3 (de)
NZ (1) NZ247939A (de)
PL (1) PL172348B1 (de)
UA (1) UA41261C2 (de)

Families Citing this family (35)

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US5606048A (en) * 1992-06-22 1997-02-25 Eli Lilly And Company Stereoselective glycosylation process for preparing 2'-Deoxy-2', 2'-difluoronucleosides and 2'-deoxy-2'-fluoronucleosides
US5424416A (en) * 1993-08-25 1995-06-13 Eli Lilly And Company Process for preparation of 2-deoxy-2,2-difluoro-D-ribofuranosyl-3,5-hydroxy protected-1-alkyl and aryl sulfonates and their use in preparation of 2',2'-difluoro-2'-deoxy nucleosides
US5637688A (en) * 1994-12-13 1997-06-10 Eli Lilly And Company Process for preparing 1-(2'-deoxy-2'-difluoro-d-ribofuranosyl)-4-aminopyrimidin-2-one hydrochloride
US5559222A (en) * 1995-02-03 1996-09-24 Eli Lilly And Company Preparation of 1-(2'-deoxy-2',2'-difluoro-D-ribo-pentofuranosyl)-cytosine from 2-deoxy-2,2-difluoro-β-D-ribo-pentopyranose
AU1289697A (en) 1995-12-13 1997-07-03 Eli Lilly And Company Alpha, alpha-difluoro-beta-hydroxy thiol esters and their synthesis
US6326507B1 (en) 1998-06-19 2001-12-04 Trustees Of Dartmouth College Therapeutic compounds and methods of use
US6949640B2 (en) * 2000-02-18 2005-09-27 Southern Research Institute Method for synthesizing 2-chloro-9-(2-fluoro-β-D-arabinofuranosyl)-9H-purin-6-amine
US7435755B2 (en) 2000-11-28 2008-10-14 The Trustees Of Dartmouth College CDDO-compounds and combination therapies thereof
DE60226447D1 (de) * 2001-08-02 2008-06-19 Ilex Oncology Inc Verfahren zur herstellung von purinnukleosiden
EP1465615B1 (de) 2002-01-15 2012-08-01 Trustees of Dartmouth College Trizyklische bisenon-derivate und verfahren zu ihrer verwendung
US6884880B2 (en) * 2002-08-21 2005-04-26 Ash Stevens, Inc. Process for the preparation of 9-β-anomeric nucleoside analogs
AU2003291726A1 (en) 2002-11-04 2004-06-07 Xenoport, Inc. Gemcitabine prodrugs, pharmaceutical compositions and uses thereof
EP1626053B1 (de) 2003-05-22 2011-07-06 Japan Science and Technology Agency Verfahren zur alpha-selektiven glycosylierung
WO2006070985A1 (en) * 2004-12-30 2006-07-06 Hanmi Pharm. Co., Ltd. METHOD FOR THE PREPARATION OF 2#-DEOXY-2#,2#-DIFLUOROCYTIDINE
BRPI0520050A2 (pt) * 2005-03-04 2009-11-17 Dabur Pharma Ltd composto, processo para a preparação de um composto e processo de glicosilação estereoseletiva para a preparação de mais de 99% de anÈmero b enriquecido de hidrocloreto de gencitabina
AU2006255706B2 (en) * 2005-06-03 2011-06-23 Scinopharm Taiwan, Ltd. Process of making an alpha-anomer enriched 2-deoxy-2,2-difluoro-d-ribofuranosyl sulfonate and use thereof for making a beta nucleoside
CN100391966C (zh) * 2005-06-17 2008-06-04 华东师范大学 一种2’-脱氧-2’，2’-二氟-胞苷合成的方法
US8921340B2 (en) 2006-11-17 2014-12-30 Trustees Of Dartmouth College Methods for using synthetic triterpenoids in the treatment of bone or cartilage diseases or conditions
WO2008064132A2 (en) 2006-11-17 2008-05-29 Trustees Of Dartmouth College Synthetic triterpenoids and tricyclic-bis-enones for use in stimulating bone and cartilage growth
US7714012B2 (en) 2006-11-17 2010-05-11 Trustees Of Dartmouth University Synthesis and biological activities of new tricyclic-bis-enones (TBEs)
US20080262215A1 (en) * 2007-04-23 2008-10-23 Chemagis Ltd. Gemcitabine production process
CN100475832C (zh) * 2007-05-31 2009-04-08 南京卡文迪许生物工程技术有限公司 一种新颖的高立体选择性合成吉西他滨工艺及中间体
EP2050757A1 (de) * 2007-10-10 2009-04-22 Cilag AG Verfahren zur Herstellung von 2' -deoxy-5-Azacytidin (Decitabin)
EP2048151A1 (de) * 2007-10-10 2009-04-15 Cilag AG Verfahren zur Herstellung von Nukleosiden durch direkte Glykosidation der Nukleosidbase
RS58486B1 (sr) 2008-01-11 2019-04-30 Reata Pharmaceuticals Inc Sintetički triterpenoidi i metode njihove upotrebe u tretmanu bolesti
RS55631B1 (sr) 2008-04-18 2017-06-30 Reata Pharmaceuticals Inc Antioksidansni modulatori upale: c-17 homologisani derivati oleanolinske kiseline
EP2279197B1 (de) 2008-04-18 2014-11-05 Reata Pharmaceuticals, Inc. Antioxidationsmittel als entzündungsmodulierende substanz: im c-ring gesättigte oleanolsäurederivate
JP5529851B2 (ja) 2008-04-18 2014-06-25 リアタ ファーマシューティカルズ インコーポレイテッド 抗酸化炎症モジュレーター：ｃ−１７においてアミノ改変およびその他の改変を加えたオレアノール酸誘導体
WO2009146216A2 (en) 2008-04-18 2009-12-03 Reata Pharmaceuticals. Inc. Antioxidant inflammation modulators: novel derivatives of oleanolic acid
MX2010011435A (es) 2008-04-18 2011-01-25 Reata Pharmaceuticals Inc Compuestos que incluyen un nucleo farmaceutico antiinflamatorio y sus metodos de uso.
US9913822B2 (en) 2012-04-04 2018-03-13 Halozyme, Inc. Combination therapy with an anti-hyaluronan agent and therapeutic agent
US8921419B2 (en) 2012-05-08 2014-12-30 Trustees Of Dartmouth College Triterpenoids and compositions containing the same
KR20150141968A (ko) * 2013-03-15 2015-12-21 에피제네틱스 파마 엘엘씨 플루오르화된 피리미딘 유사체 및 그의 사용 방법
WO2018200859A1 (en) 2017-04-26 2018-11-01 Kalman Thomas I Multitargeted nucleoside derivatives
US20190351031A1 (en) 2018-05-16 2019-11-21 Halozyme, Inc. Methods of selecting subjects for combination cancer therapy with a polymer-conjugated soluble ph20

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA1295998C (en) * 1985-07-29 1992-02-18 Sai P. Sunkara Nucleosides and their use as antineoplastic agents
DE3856158T2 (de) * 1987-08-28 1998-08-20 Lilly Co Eli Verfahren zur Herstellung von Zwischenverbindungen verwendbar in der Herstellung von 2',2'-Difluoronucleosiden
JPH0217199A (ja) * 1988-07-05 1990-01-22 Japan Tobacco Inc ２’−デオキシ−β−アデノシンの製造方法
GB8816345D0 (en) * 1988-07-08 1988-08-10 Hoffmann La Roche Purine derivatives
HU906976D0 (en) * 1989-11-13 1991-05-28 Bristol Myers Squibb Co Process for producing 2', 3'-didesoxy-2'-fluoarabinonucleoside analogues
WO1991015498A2 (en) * 1990-04-04 1991-10-17 Nycomed Imaging As Nucleoside derivatives
US5817799A (en) * 1990-07-23 1998-10-06 The United States Of America As Represented By The Department Of Health And Human Services 2'-Fluorofuranosyl derivatives and methods for preparing 2'-fluoropyrimidine and 2'-fluoropurine nucleosides
US5256798A (en) * 1992-06-22 1993-10-26 Eli Lilly And Company Process for preparing alpha-anomer enriched 2-deoxy-2,2-difluoro-D-ribofuranosyl sulfonates
US5371210A (en) * 1992-06-22 1994-12-06 Eli Lilly And Company Stereoselective fusion glycosylation process for preparing 2'-deoxy-2',2'-difluoronucleosides and 2'-deoxy-2'-fluoronucleosides

Also Published As

Publication number Publication date
KR940005658A (ko) 1994-03-22
MY115775A (en) 2003-09-30
DE69314239T2 (de) 1998-02-19
FI108643B (fi) 2002-02-28
HU0201196D0 (de) 2002-06-29
HU223837B1 (hu) 2005-02-28
NO932288A (no) 1993-12-23
GR3025689T3 (en) 1998-03-31
ATE158799T1 (de) 1997-10-15
IL106071A0 (en) 1993-10-20
PL172348B1 (pl) 1997-09-30
PL299415A1 (en) 1994-03-07
ES2107624T3 (es) 1997-12-01
NO180235B3 (no) 2007-10-01
BR9302434A (pt) 1994-02-16
FI932869A0 (fi) 1993-06-21
JP3313191B2 (ja) 2002-08-12
NO932288D0 (no) 1993-06-21
CY2067A (en) 1993-06-21
FI932869A (fi) 1993-12-23
NZ247939A (en) 1996-02-27
NO180235C (no) 1997-03-12
DK0577303T3 (da) 1997-10-27
HUT64358A (en) 1993-12-28
KR100252452B1 (en) 2000-04-15
DE69314239C5 (de) 2012-11-29
HU9301822D0 (en) 1993-09-28
IL106071A (en) 2006-08-20
CA2098881A1 (en) 1993-12-23
EP0577303A1 (de) 1994-01-05
EP0577303B1 (de) 1997-10-01
JPH06157570A (ja) 1994-06-03
CA2098881C (en) 2005-06-07
MX9303707A (es) 1994-06-30
NO180235B (no) 1996-12-02
UA41261C2 (uk) 2001-09-17

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Legal Events

Date Code Title Description
8364 No opposition during term of opposition
8310 Action for declaration of annulment
8328 Change in the person/name/address of the agent

Representative=s name: KOENIG SZYNKA TILMANN VON RENESSE, 40549 DUESSELDO

R206 Amended patent specification

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