UY23910A1 - Procedimiento para la preparacion de 5- derivados sustitutivos del acido micofenolico - Google Patents

Procedimiento para la preparacion de 5- derivados sustitutivos del acido micofenolico

Info

Publication number
UY23910A1
UY23910A1 UY23910A UY23910A UY23910A1 UY 23910 A1 UY23910 A1 UY 23910A1 UY 23910 A UY23910 A UY 23910A UY 23910 A UY23910 A UY 23910A UY 23910 A1 UY23910 A1 UY 23910A1
Authority
UY
Uruguay
Prior art keywords
mycophenolic acid
procedure
preparation
substitute derivatives
derivatives
Prior art date
Application number
UY23910A
Other languages
English (en)
Inventor
R Elworthy Todd
G Loughhead David
H Nelson Peter
B Sjogren Eric
Marie Waltos Ann
F Andrade Fidencio
X T Murra Francisco
C Rohloff John
B Smith David
J Weikert Robert
F Zertuche Mario
A T Martin Teresa
R Artis Dean
C Hawley Ronald
J Morgans David Jr
W Patterson John Jr
C García Alicia
T L Hernández Maria
Original Assignee
Syntex 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 Syntex Inc filed Critical Syntex Inc
Publication of UY23910A1 publication Critical patent/UY23910A1/es

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    • 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 Table
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Transplantation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

Se describe un proceso para la preparación de un compuesto de fórmula I (figura 1) donde R1 es hidrógeno o C(O)R10 donde R10 es alquilo inferior, arilo o NH-arilo; y Z se selecciona de, por ejemplo, la fórmula ZA (figura 2) donde Z13 es heteroarilo, entre otras posibilidades; Z3 o Z4 tomados juntos con el carbono al cual están uniodos forman cicloalquilo de 3 a 5 átomos de carbonos; o una sal farmaceuticamente aceptable, cuyo proceso comprende: (a) desprotegiendo un compuesto de Fórmula I'; (b) hidrolizando un compuesto de Fórmula I; (c) esterificando un compuesto de Fórmula I; (d) oxidando un compuesto de Fórmula I; (e) reduciendo un compuesto de Fórmula I'; (f) decarboxilando un compuesto de Fórmula I' (g) convirtiendo un compuesto libre de fórmula I con un reactivo en un solvente bajo una temperatura que se sabe es adecuada para la preparación de una sal, para formar una sal farmaceuticamente aceptable del compuesto de Fórmula I. Como ejemplo no limitante: (+) (E)-6-(1,3-dihidro-4-hidroxi-6-metoxi-7-metilo-3-oxoisobenzufurano-5-yl)-2,3,4-trimetil-4-acido hexonoico. Son agentes terapéuticos ventajosos en el tratamiento de enfermedades indicados para el ácido micofenólico y/o micofenolato mofetil, incluyendo inmunidad, inflamación, tumores, proliferantes, virosos o desórdenes psoriáticos.
UY23910A 1994-02-18 1995-02-16 Procedimiento para la preparacion de 5- derivados sustitutivos del acido micofenolico UY23910A1 (es)

Applications Claiming Priority (1)

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

Publications (1)

Publication Number Publication Date
UY23910A1 true UY23910A1 (es) 1995-03-06

Family

ID=22734662

Family Applications (2)

Application Number Title Priority Date Filing Date
UY23910A UY23910A1 (es) 1994-02-18 1995-02-16 Procedimiento para la preparacion de 5- derivados sustitutivos del acido micofenolico
UY25262A UY25262A1 (es) 1994-02-18 1998-11-23 5-derivados sustituidos del ácido micofenolico

Family Applications After (1)

Application Number Title Priority Date Filing Date
UY25262A UY25262A1 (es) 1994-02-18 1998-11-23 5-derivados sustituidos del ácido micofenolico

Country Status (29)

Country Link
US (2) US5493030A (es)
EP (1) EP0745073B1 (es)
JP (1) JPH09509174A (es)
CN (1) CN1141038A (es)
AT (1) ATE194608T1 (es)
AU (1) AU1875495A (es)
BR (1) BR9506819A (es)
CA (1) CA2183530A1 (es)
CO (1) CO4340734A1 (es)
DE (1) DE69517957T2 (es)
DK (1) DK0745073T3 (es)
ES (1) ES2149971T3 (es)
FI (1) FI963218A (es)
GR (1) GR3033864T3 (es)
GT (1) GT199500007A (es)
HR (1) HRP950070B1 (es)
IL (2) IL112665A (es)
IS (1) IS4264A (es)
MX (1) MX9603478A (es)
MY (1) MY112804A (es)
PE (1) PE22996A1 (es)
PH (1) PH31441A (es)
PT (1) PT745073E (es)
SI (1) SI0745073T1 (es)
SV (1) SV1995000007A (es)
TW (1) TW384288B (es)
UY (2) UY23910A1 (es)
WO (1) WO1995022538A1 (es)
ZA (1) ZA951299B (es)

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US7179791B2 (en) 2001-01-11 2007-02-20 Duke University Inhibiting GS-FDH to modulate NO bioactivity
US20040127435A1 (en) * 2002-08-02 2004-07-01 Regents Of The University Of California Uses for inhibitors of inosine monophosphate dehydrogenase
WO2004096287A2 (en) * 2003-04-25 2004-11-11 Gilead Sciences, Inc. Inosine monophosphate dehydrogenase inhibitory phosphonate compounds
JP2006524710A (ja) * 2003-04-25 2006-11-02 ギリアード サイエンシーズ, インコーポレイテッド キナーゼインヒビターホスホネート抱合体
CN101410120A (zh) * 2003-04-25 2009-04-15 吉里德科学公司 抗炎的膦酸酯化合物
US20050261237A1 (en) * 2003-04-25 2005-11-24 Boojamra Constantine G Nucleoside phosphonate analogs
US7470724B2 (en) * 2003-04-25 2008-12-30 Gilead Sciences, Inc. Phosphonate compounds having immuno-modulatory activity
US7452901B2 (en) * 2003-04-25 2008-11-18 Gilead Sciences, Inc. Anti-cancer phosphonate analogs
US20090247488A1 (en) * 2003-04-25 2009-10-01 Carina Cannizzaro Anti-inflammatory phosphonate compounds
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DK1628685T3 (da) * 2003-04-25 2011-03-21 Gilead Sciences Inc Antivirale phosphonatanaloge
US7407965B2 (en) * 2003-04-25 2008-08-05 Gilead Sciences, Inc. Phosphonate analogs for treating metabolic diseases
US20050187170A1 (en) * 2003-06-16 2005-08-25 Biocryst Pharmaceuticals, Inc. Enhancing the efficiency of RNA polymerase inhibitors by using inosine monophosphate dehydrogenase inhibitors
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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
MXPA06006899A (es) * 2003-12-22 2006-09-04 Gilead Sciences Inc Derivados de carbovir y abacavir 4'-sustituidos asi como compuestos relacionados con actividad antiviral de virus de inmunodeficiencia humana y virus de la hepatitis c.
US20070281907A1 (en) * 2003-12-22 2007-12-06 Watkins William J Kinase Inhibitor Phosphonate Conjugates
US20050153990A1 (en) * 2003-12-22 2005-07-14 Watkins William J. Phosphonate substituted kinase inhibitors
CA2571710A1 (en) 2004-06-24 2006-11-02 Nicholas Valiante Small molecule immunopotentiators and assays for their detection
US7871991B2 (en) 2004-07-27 2011-01-18 Gilead Sciences, Inc. Phosphonate analogs of HIV inhibitor compounds
CA2585353A1 (en) * 2004-10-26 2006-05-04 Gilead Sciences, Inc. Phosphonate derivatives of mycophenolic acid
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
MX2011000306A (es) * 2008-07-08 2011-03-15 Gilead Sciences Inc Sales de compuestos inhibidores de hiv.
WO2013044028A2 (en) * 2011-09-21 2013-03-28 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
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US10603299B2 (en) 2016-06-02 2020-03-31 Steven Baranowitz Prevention and treatment of viral infections
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Also Published As

Publication number Publication date
PT745073E (pt) 2000-12-29
EP0745073A1 (en) 1996-12-04
DK0745073T3 (da) 2000-09-18
PE22996A1 (es) 1996-06-04
MX9603478A (es) 1997-12-31
DE69517957D1 (de) 2000-08-17
IL124139A (en) 2000-02-29
GR3033864T3 (en) 2000-10-31
FI963218A (fi) 1996-10-11
MY112804A (en) 2001-09-29
HRP950070A2 (en) 1997-06-30
ES2149971T3 (es) 2000-11-16
CA2183530A1 (en) 1995-08-24
ZA951299B (en) 1996-08-16
FI963218A0 (fi) 1996-08-16
CN1141038A (zh) 1997-01-22
AU1875495A (en) 1995-09-04
IL112665A (en) 1999-05-09
TW384288B (en) 2000-03-11
PH31441A (en) 1998-11-03
SV1995000007A (es) 1996-02-28
BR9506819A (pt) 1997-09-09
UY25262A1 (es) 2001-01-31
JPH09509174A (ja) 1997-09-16
US5633279A (en) 1997-05-27
WO1995022538A1 (en) 1995-08-24
IS4264A (is) 1995-08-19
US5493030A (en) 1996-02-20
SI0745073T1 (en) 2000-12-31
DE69517957T2 (de) 2001-01-25
ATE194608T1 (de) 2000-07-15
CO4340734A1 (es) 1996-07-30
GT199500007A (es) 1996-08-10
IL112665A0 (en) 1995-05-26
EP0745073B1 (en) 2000-07-12
HRP950070B1 (en) 2001-02-28

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