DE69517957D1 - 5-substituierte derivate von mycophenolsäure - Google Patents

5-substituierte derivate von mycophenolsäure

Info

Publication number
DE69517957D1
DE69517957D1 DE69517957T DE69517957T DE69517957D1 DE 69517957 D1 DE69517957 D1 DE 69517957D1 DE 69517957 T DE69517957 T DE 69517957T DE 69517957 T DE69517957 T DE 69517957T DE 69517957 D1 DE69517957 D1 DE 69517957D1
Authority
DE
Germany
Prior art keywords
mycophenolic acid
substituted derivatives
acid
proliferative
viral
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 - Fee Related
Application number
DE69517957T
Other languages
English (en)
Other versions
DE69517957T2 (de
Inventor
R Artis
R Elworthy
C Hawley
G Loughhead
J Morgans
H Nelson
W Patterson
C Rohloff
B Sjogren
B Smith
Marie Waltos
J Weikert
C Garcia
F Zertuche
F Andrade
T Hernandez
X Murra
A Martin
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.)
Syntex USA LLC
Original Assignee
Syntex USA LLC
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 Syntex USA LLC filed Critical Syntex USA LLC
Application granted granted Critical
Publication of DE69517957D1 publication Critical patent/DE69517957D1/de
Publication of DE69517957T2 publication Critical patent/DE69517957T2/de
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/06Heterocyclic 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 carbon chain containing only aliphatic carbon atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D307/00Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/77Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D307/87Benzo [c] furans; Hydrogenated benzo [c] furans
    • C07D307/88Benzo [c] furans; Hydrogenated benzo [c] furans with one oxygen atom directly attached in position 1 or 3
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D407/00Heterocyclic 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
    • C07D407/02Heterocyclic 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
    • C07D407/06Heterocyclic 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 linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/06Heterocyclic 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 carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic System
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/655Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having oxygen atoms, with or without sulfur, selenium, or tellurium atoms, as the only ring hetero atoms
    • C07F9/65515Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having oxygen atoms, with or without sulfur, selenium, or tellurium atoms, as the only ring hetero atoms the oxygen atom being part of a five-membered ring
    • C07F9/65517Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having oxygen atoms, with or without sulfur, selenium, or tellurium atoms, as the only ring hetero atoms the oxygen atom being part of a five-membered ring condensed with carbocyclic rings or carbocyclic ring systems
DE69517957T 1994-02-18 1995-02-16 5-substituierte derivate von mycophenolsäure Expired - Fee Related DE69517957T2 (de)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US08/198,749 US5493030A (en) 1994-02-18 1994-02-18 5-substituted derivatives of mycophenolic acid
PCT/US1995/001787 WO1995022538A1 (en) 1994-02-18 1995-02-16 5-substituted derivatives of mycophenolic acid

Publications (2)

Publication Number Publication Date
DE69517957D1 true DE69517957D1 (de) 2000-08-17
DE69517957T2 DE69517957T2 (de) 2001-01-25

Family

ID=22734662

Family Applications (1)

Application Number Title Priority Date Filing Date
DE69517957T Expired - Fee Related DE69517957T2 (de) 1994-02-18 1995-02-16 5-substituierte derivate von mycophenolsäure

Country Status (29)

Country Link
US (2) US5493030A (de)
EP (1) EP0745073B1 (de)
JP (1) JPH09509174A (de)
CN (1) CN1141038A (de)
AT (1) ATE194608T1 (de)
AU (1) AU1875495A (de)
BR (1) BR9506819A (de)
CA (1) CA2183530A1 (de)
CO (1) CO4340734A1 (de)
DE (1) DE69517957T2 (de)
DK (1) DK0745073T3 (de)
ES (1) ES2149971T3 (de)
FI (1) FI963218A (de)
GR (1) GR3033864T3 (de)
GT (1) GT199500007A (de)
HR (1) HRP950070B1 (de)
IL (2) IL124139A (de)
IS (1) IS4264A (de)
MX (1) MX9603478A (de)
MY (1) MY112804A (de)
PE (1) PE22996A1 (de)
PH (1) PH31441A (de)
PT (1) PT745073E (de)
SI (1) SI0745073T1 (de)
SV (1) SV1995000007A (de)
TW (1) TW384288B (de)
UY (2) UY23910A1 (de)
WO (1) WO1995022538A1 (de)
ZA (1) ZA951299B (de)

Families Citing this family (35)

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US6514979B1 (en) * 1999-03-03 2003-02-04 University Of Maryland Biotechnology Institute Synergistic combinations of guanosine analog reverse transcriptase inhibitors and inosine monophosphate dehydrogenese inhibitors and uses therefor
US6811998B2 (en) * 1999-06-25 2004-11-02 Roche Diagnostics Operations, Inc. Conjugates of uncompetitive inhibitors of inosine monophosphate dehydrogenase
US7214754B2 (en) * 1999-12-13 2007-05-08 Ppg Industries Ohio, Inc. Polymerizable polyol (allyl carbonate) compositions
US7179791B2 (en) * 2001-01-11 2007-02-20 Duke University Inhibiting GS-FDH to modulate NO bioactivity
AU2003261354A1 (en) * 2002-08-02 2004-02-23 The Regents Of The University Of California New uses for inhibitors of inosine monophosphate dehydrogenase
US20050261237A1 (en) * 2003-04-25 2005-11-24 Boojamra Constantine G Nucleoside phosphonate analogs
ATE490788T1 (de) 2003-04-25 2010-12-15 Gilead Sciences Inc Antivirale phosphonate analoge
US7452901B2 (en) * 2003-04-25 2008-11-18 Gilead Sciences, Inc. Anti-cancer phosphonate analogs
WO2005002626A2 (en) 2003-04-25 2005-01-13 Gilead Sciences, Inc. Therapeutic phosphonate compounds
WO2004096285A2 (en) * 2003-04-25 2004-11-11 Gilead Sciences, Inc. Anti-infective phosphonate conjugates
US7470724B2 (en) * 2003-04-25 2008-12-30 Gilead Sciences, Inc. Phosphonate compounds having immuno-modulatory activity
US7407965B2 (en) * 2003-04-25 2008-08-05 Gilead Sciences, Inc. Phosphonate analogs for treating metabolic diseases
US20090247488A1 (en) * 2003-04-25 2009-10-01 Carina Cannizzaro Anti-inflammatory phosphonate compounds
CN101410120A (zh) * 2003-04-25 2009-04-15 吉里德科学公司 抗炎的膦酸酯化合物
WO2004096287A2 (en) * 2003-04-25 2004-11-11 Gilead Sciences, Inc. Inosine monophosphate dehydrogenase inhibitory phosphonate compounds
US7432261B2 (en) * 2003-04-25 2008-10-07 Gilead Sciences, Inc. Anti-inflammatory phosphonate compounds
EA200501676A1 (ru) * 2003-04-25 2006-04-28 Джилид Сайэнс, Инк. Фосфонатсодержащие ингибиторы киназы (варианты), способ их получения, фармацевтическая композиция, лекарственная форма на их основе и способ ингибирования киназы у млекопитающего (варианты)
US20050187170A1 (en) * 2003-06-16 2005-08-25 Biocryst Pharmaceuticals, Inc. Enhancing the efficiency of RNA polymerase inhibitors by using inosine monophosphate dehydrogenase inhibitors
US20070032483A1 (en) * 2003-09-11 2007-02-08 Julia Greil Process for the production of mycophenolate mofetil
WO2005044279A1 (en) * 2003-10-24 2005-05-19 Gilead Sciences, Inc. Purine nucleoside phosphonate conjugates
WO2005044308A1 (en) * 2003-10-24 2005-05-19 Gilead Sciences, Inc. Phosphonate analogs of antimetabolites
JP2007515495A (ja) * 2003-12-22 2007-06-14 ギリアード サイエンシーズ, インコーポレイテッド 4’−置換カルボビル誘導体およびアバカビル誘導体ならびにhivおよびhcv抗ウイルス活性を有する関連化合物
US20050153990A1 (en) * 2003-12-22 2005-07-14 Watkins William J. Phosphonate substituted kinase inhibitors
BRPI0418031A (pt) * 2003-12-22 2007-04-17 Gilead Sciences Inc inibidores de quinase fosfonato-substituìdos
CA2571710A1 (en) 2004-06-24 2006-11-02 Nicholas Valiante Small molecule immunopotentiators and assays for their detection
TR201906416T4 (tr) 2004-07-27 2019-05-21 Gilead Sciences Inc Hiv inhibitörü bileşiklerin fosfonat analogları.
EP1809277A2 (de) * 2004-10-26 2007-07-25 Inc. Gilead Sciences Phosphonatderivate aus mycophenolsäure
WO2008033466A2 (en) * 2006-09-14 2008-03-20 Combinatorx (Singapore) Pre. Ltd. Compositions and methods for treatment of viral diseases
CN101422424B (zh) * 2007-10-31 2012-10-24 王世亮 霉酚酸类药物植入剂及其制备方法和应用
PE20110219A1 (es) 2008-07-08 2011-03-31 Gilead Sciences Inc Sales del compuesto n-[(s)({[(2r,5r)-5-(6-amino-9h-purin-9-il)-4-fluoro-2,5-dihidrofuran-2-il]oxi}metil)fenoxifosfinoil]-l-alaninato de etilo como inhibidores de vih
US9492426B2 (en) * 2011-09-21 2016-11-15 The Texas A&M University System Mycophenolic acid analogues as anti-tumor chemosensitizing agents
CN105271935B (zh) * 2015-11-03 2017-06-30 陶祖岐 一种生活垃圾制成的装饰板和包装箱板
WO2017210262A1 (en) 2016-06-02 2017-12-07 Steven Baranowitz Prevention and treatment of viral infections
US10603299B2 (en) 2016-06-02 2020-03-31 Steven Baranowitz Prevention and treatment of viral infections
PL3661937T3 (pl) 2017-08-01 2021-12-20 Gilead Sciences, Inc. Formy krystaliczne ((s)-((((2r,5r)-5-(6-amino-9h-puryn-9-ylo)-4-fluoro-2,5-dihydrofuran-2-ylo)oksy)metylo)(fenoksy)fosforylo)-l-alaninianu etylu (gs-9131) do leczenia zakażeń wirusowych

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US3825571A (en) * 1971-07-31 1974-07-23 Chugai Pharmaceutical Co Ltd Mycophenolic acid derivatives
JPS5542995B2 (de) * 1972-02-24 1980-11-04
JPS5529994B2 (de) * 1972-03-02 1980-08-07
US4515956A (en) * 1982-12-16 1985-05-07 The Dow Chemical Company Selective preparation of isomers and enantiomers of cyclopropane carboxylic acids
US4479005A (en) * 1982-12-16 1984-10-23 The Dow Chemical Company Selective preparation of isomers and enantiomers of cyclopropane carboxylic acids
US4686234A (en) * 1985-11-27 1987-08-11 Syntex (U.S.A) Inc. Mycophenolic acid derivatives in the treatment of inflammatory diseases, in particular rheumatoid arthritis
US4725622A (en) * 1986-01-23 1988-02-16 Syntex (U.S.A.) Inc. Mycophenolic acid derivatives in the treatment of rheumatoid arthritis
US4959387A (en) * 1986-01-23 1990-09-25 Syntex (U.S.A.) Inc. Mycophenolic acid derivatives in the treatment of rheumatoid arthritis
US5231179A (en) * 1986-01-27 1993-07-27 Sumitomo Pharmaceuticals Company, Limited Heterocyclic compounds and their production
US4753935A (en) * 1987-01-30 1988-06-28 Syntex (U.S.A.) Inc. Morpholinoethylesters of mycophenolic acid and pharmaceutical compositions
US4727069A (en) * 1987-01-30 1988-02-23 Syntex (U.S.A.) Inc. Heterocyclic aminoalkyl esters of mycophenolic acid, derivatives thereof and pharmaceutical compositions
US4861776A (en) * 1987-01-30 1989-08-29 Syntex (U.S.A) Inc. Heterocyclic aminoalkyl esters of mycophenolic acid and derivatives thereof, compositions and use
US4748173A (en) * 1987-01-30 1988-05-31 Syntex (U.S.A.) Inc. Heterocyclic aminoalkyl esters of mycophenolic acid and derivatives thereof and pharmaceutical compositions
JPH0637486B2 (ja) * 1988-05-18 1994-05-18 三共株式会社 新規抗生物質フタレキシンおよびその製造法
US4940797A (en) * 1989-03-23 1990-07-10 Merck & Co., Inc. Process for synthesis of FK-506 C10-C18 intermediates
US5155228A (en) * 1989-03-23 1992-10-13 Merck & Co., Inc. FK-506 C10-C18 process intermediates
US5068345A (en) * 1989-10-30 1991-11-26 Eastman Kodak Company Oxazolidinone aldol adduct
US5247083A (en) * 1992-07-10 1993-09-21 Syntex (U.S.A.) Inc. Direct esterification of mycophenolic acid

Also Published As

Publication number Publication date
UY23910A1 (es) 1995-03-06
FI963218A0 (fi) 1996-08-16
PH31441A (en) 1998-11-03
WO1995022538A1 (en) 1995-08-24
IL112665A (en) 1999-05-09
JPH09509174A (ja) 1997-09-16
UY25262A1 (es) 2001-01-31
PT745073E (pt) 2000-12-29
SV1995000007A (es) 1996-02-28
DE69517957T2 (de) 2001-01-25
EP0745073B1 (de) 2000-07-12
AU1875495A (en) 1995-09-04
FI963218A (fi) 1996-10-11
ZA951299B (en) 1996-08-16
CA2183530A1 (en) 1995-08-24
GR3033864T3 (en) 2000-10-31
CN1141038A (zh) 1997-01-22
EP0745073A1 (de) 1996-12-04
US5633279A (en) 1997-05-27
GT199500007A (es) 1996-08-10
TW384288B (en) 2000-03-11
MY112804A (en) 2001-09-29
HRP950070A2 (en) 1997-06-30
BR9506819A (pt) 1997-09-09
IL112665A0 (en) 1995-05-26
HRP950070B1 (en) 2001-02-28
PE22996A1 (es) 1996-06-04
ES2149971T3 (es) 2000-11-16
US5493030A (en) 1996-02-20
MX9603478A (es) 1997-12-31
ATE194608T1 (de) 2000-07-15
DK0745073T3 (da) 2000-09-18
SI0745073T1 (en) 2000-12-31
IS4264A (is) 1995-08-19
IL124139A (en) 2000-02-29
CO4340734A1 (es) 1996-07-30

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Legal Events

Date Code Title Description
8364 No opposition during term of opposition
8339 Ceased/non-payment of the annual fee