CO4340735A1 - Acido micofenolico 6-sustituido y derivados y procedimiento para su preparacion - Google Patents

Acido micofenolico 6-sustituido y derivados y procedimiento para su preparacion

Info

Publication number
CO4340735A1
CO4340735A1 CO95005931A CO95005931A CO4340735A1 CO 4340735 A1 CO4340735 A1 CO 4340735A1 CO 95005931 A CO95005931 A CO 95005931A CO 95005931 A CO95005931 A CO 95005931A CO 4340735 A1 CO4340735 A1 CO 4340735A1
Authority
CO
Colombia
Prior art keywords
mycophenolic acid
derivatives
procedure
preparation
substituted mycophenolic
Prior art date
Application number
CO95005931A
Other languages
English (en)
Inventor
Dean R Artis
Todd R Elworthy
Ronald C Hawley
David G Loughhead
David J Morgans
Jr Nelson Peter H
John W Patterson
Eric B Sjogren Jr
David B Smith
Ann Marie Waltos
Robert J Weikert
Alicia C Garcia
Mario F Zertuche
Fidencio F Andrade
Maria T L Hernandez
Francisco Xt Murra
Teresa A T Martin
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 CO4340735A1 publication Critical patent/CO4340735A1/es

Links

Classifications

    • 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
    • C07D307/78Benzo [b] furans; Hydrogenated benzo [b] furans
    • C07D307/82Benzo [b] furans; Hydrogenated benzo [b] furans 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 carbon atoms of the hetero ring
    • C07D307/83Oxygen 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (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)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Transplantation (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Dermatology (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

REIVINDICACION NUMERO UN COMPUESTO DE FORMULA FIGURA 1 EN DONDE: R1 ES H o C(O)R10, EN DONDE R10 ES UN ALQUILO INFERIOR, ARILO O NH-ARILO; R2 ES ALQUILO INFERIOR, CICLOALQUILO, VINILO, FLUOROVINILO, DIFLUOROVINILO, TRIFLUOROVINILO, AL- QUENILO, -C=C-R11, ALENILO, CHO O CH2OR12, EN DONDE R11 ES H O ALQUILO INFERIOR, Y R12 ES H o 4-METOXIBENCILO; Y Z ES UNA CADENA LATERAL SELECCIONADA DE LA FORMULA ZA, ZB, ZC, ZD, ZE, ZF, ZG, Y ZH: FIGURA 2 EN DONDE: Z1 ES H, ALQUILO INFERIOR, HALO O CF3; Z2 ES H, ALQUILO INFERIOR, ALCOXI INFERIOR, ARILO, O CH2-Z11, EN DONDE Z11 ES HALO, CN, ARILO O HETEROARILO; Z3 ES H, ALQUILO INFERIOR, ALQUENILO INFERIOR, AL- COXI INFERIOR, FENILO O ALQUILO -S(O)n INFERIOR, EN DONDE m ES 0, 1 o 2; Z4 ES H, ALQUILO INFERIOR O FENILO; o Z3 y Z4 TOMADOS JUNTOS CON EL CARBON AL CUAL ES- TAN UNIDOS FORMAN UN CICLO ALQUILO DE 3 A 5 ATOMOS DE CARBON; Y G ES OH, ALCOXI INFERIOR, TIOALQUILO INFERIOR NG1G2, O-(CH2)n-NG1G2 o O-(CH2)n-N=G3, EN DONDE n ES UN ENTERO ENTRE 1 Y 6, G1 ES H o ALQUILO INFERIOR, G2 ES H o ALQUILO INFERIOR, Y =G3 ES ALQUILENO INFERIOR DE 4 A 6 ATOMOS DE CAR- BON, O ALQUILENO INFERIOR DE 3 A 5 ATOMOS DE CAR- BON MAS UN MIEMBRO QUE ES -O-, -S-, o -N(G)- EN DONDE G4 ES H o ALQUILO INFERIOR; O FIGURA 3 EN DONDE Z5 ES H, O ALQUILO INFERIOR; Z8 ES H, ALQUILO INFERIOR O FORMA UN DOBLE ENLACE CON D2; D1 y D2 JUNTO CON SU ATOMOS DE CARBON ADYACENTES FORMAN UN ANILLO OPCIONALMENTE SUSTITUIDO, SATURA- DO O INSATURADO, CARBOXICLICO O HETEROCICLICO DE 3 A 7 ATOMOS; y G ES COMO SE DEFINIO ANTERIORMENTE; O FIGURA 4 EN DONDE: Z8 ES H o ALQUILO INFERIOR; Y Z5 y G SON COMO SE DEFINIERON ANTERIORMENTE; O FIGURA 5 EN DONDE: D3 ES -CH2- o -CH2-CH2-; Y G ES COMO SE DEFINIO ANTERIORMENTE; O FIGURA 6 EN DONDE: Z6 ES H, ALQUILO INFERIOR, COOH, NH2, ACIDO O HALO Z7 ES H, ALQUILO INFERIOR O HALO; Y Z5 y G SON COMO SE DEFINIERON ANTERIORMENTE; O FIGURA 7 EN DONDE: Z1 y G SON COMO SE DEFINIERON ANTERIORMENTE; O FIGURA 8 D3, Z2, Z3, Z4 y G SON COMO SE DEFINIERON ANTE- RIORMENTE; O FIGURA 9 EN DONDE: D4 ES -CH2-, -CH2-CH2-, -CH2-CH2-CH2-, -O-, o -O-CH2-; Y Z1 y G SON COMO SE DEFINIERON ANTERIORMENTE; Y LAS SALES DE ELLOS FARMACEUTICAMENTE ACEPTABLES.
CO95005931A 1994-02-18 1995-02-16 Acido micofenolico 6-sustituido y derivados y procedimiento para su preparacion CO4340735A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US08/198,725 US5444072A (en) 1994-02-18 1994-02-18 6-substituted mycophenolic acid and derivatives

Publications (1)

Publication Number Publication Date
CO4340735A1 true CO4340735A1 (es) 1996-07-30

Family

ID=22734546

Family Applications (1)

Application Number Title Priority Date Filing Date
CO95005931A CO4340735A1 (es) 1994-02-18 1995-02-16 Acido micofenolico 6-sustituido y derivados y procedimiento para su preparacion

Country Status (28)

Country Link
US (2) US5444072A (es)
EP (1) EP0745075B1 (es)
JP (1) JPH09509172A (es)
CN (1) CN1141040A (es)
AT (1) ATE210127T1 (es)
AU (1) AU1917095A (es)
BR (1) BR9506835A (es)
CA (1) CA2183533A1 (es)
CO (1) CO4340735A1 (es)
DE (1) DE69524389T2 (es)
DK (1) DK0745075T3 (es)
ES (1) ES2168359T3 (es)
FI (1) FI963221A (es)
GT (1) GT199500006A (es)
HK (1) HK1012634A1 (es)
HR (1) HRP950071A2 (es)
IL (1) IL112667A (es)
IS (1) IS4265A (es)
MY (1) MY130110A (es)
PE (1) PE23096A1 (es)
PH (1) PH31406A (es)
PT (1) PT745075E (es)
SI (1) SI0745075T1 (es)
SV (1) SV1995000006A (es)
TW (1) TW369532B (es)
UY (2) UY23909A1 (es)
WO (1) WO1995022536A1 (es)
ZA (1) ZA951295B (es)

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US6054472A (en) * 1996-04-23 2000-04-25 Vertex Pharmaceuticals, Incorporated Inhibitors of IMPDH enzyme
US5807876A (en) * 1996-04-23 1998-09-15 Vertex Pharmaceuticals Incorporated Inhibitors of IMPDH enzyme
SK286662B6 (sk) 1996-04-23 2009-03-05 Vertex Pharmaceuticals Incorporated Deriváty močoviny, farmaceutické prostriedky, ktoré ich obsahujú, a ich použitie ako inhibítorov aktivity IMPDH enzýmu
US6128582A (en) * 1996-04-30 2000-10-03 Vertex Pharmaceuticals Incorporated Molecules comprising an IMPDH-like binding pocket and encoded data storage medium capable of graphically displaying them
EP1366766A1 (en) * 1997-03-14 2003-12-03 Vertex Pharmaceuticals Incorporated Inhibitors of IMPDH enzyme
ES2201452T3 (es) * 1997-03-14 2004-03-16 Vertex Pharmaceuticals Incorporated Inhibidores de la enzima impdh.
US5932600A (en) * 1997-03-14 1999-08-03 Vertex Pharmaceuticals Incorporated Inhibitors of IMPDH enzyme
WO2000015210A2 (en) * 1998-09-14 2000-03-23 Vertex Pharmaceuticals Incorporated Use of mycophenol acid and its derivatives for the treatment of virus diseases
US6596747B2 (en) 1998-10-29 2003-07-22 Bristol-Myers Squibb Company Compounds derived from an amine nucleus and pharmaceutical compositions comprising same
WO2000026197A1 (en) * 1998-10-29 2000-05-11 Bristol-Myers Squibb Company Novel inhibitors of impdh enzyme
WO2000025780A1 (en) 1998-10-29 2000-05-11 Bristol-Myers Squibb Company Compounds derived from an amine nucleus that are inhibitors of impdh enzyme
US6420403B1 (en) 1998-10-29 2002-07-16 Edwin J. Iwanowicz Inhibitors of IMPDH enzyme
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
EP1964561A1 (en) 1999-03-19 2008-09-03 Vertex Pharmaceuticals Incorporated Inhibitors of IMPDH enzyme
US6107052A (en) * 1999-06-09 2000-08-22 Roche Diagnostics Corporation Enzymatic measurement of mycophenolic acid
US6811998B2 (en) 1999-06-25 2004-11-02 Roche Diagnostics Operations, Inc. Conjugates of uncompetitive inhibitors of inosine monophosphate dehydrogenase
ATE248835T1 (de) 1999-06-25 2003-09-15 Vertex Pharma Prodrugs von impdh-inhibierenden carbamaten
EP1276739A2 (en) * 2000-04-24 2003-01-22 Bristol-Myers Squibb Company Heterocycles that are inhibitors of impdh enzyme
US7179791B2 (en) * 2001-01-11 2007-02-20 Duke University Inhibiting GS-FDH to modulate NO bioactivity
WO2003035066A1 (en) * 2001-10-23 2003-05-01 Celltech R & D Limited 2-aminoquinolone derivatives for use as impdh inhibitors
TW200301698A (en) * 2001-12-21 2003-07-16 Bristol Myers Squibb Co Acridone inhibitors of IMPDH enzyme
EP2181704B1 (en) 2002-12-30 2015-05-06 Angiotech International Ag Drug delivery from rapid gelling polymer composition
US20050187170A1 (en) * 2003-06-16 2005-08-25 Biocryst Pharmaceuticals, Inc. Enhancing the efficiency of RNA polymerase inhibitors by using inosine monophosphate dehydrogenase inhibitors
US7276362B2 (en) 2004-01-30 2007-10-02 Roche Diagnostics Operations, Inc. Recombinant histidine-tagged inosine monophosphate dehydrogenase polypeptides
CA2571710A1 (en) 2004-06-24 2006-11-02 Nicholas Valiante Small molecule immunopotentiators and assays for their detection
CN102952105A (zh) * 2011-08-26 2013-03-06 中国科学院上海药物研究所 一类霉酚酸衍生物、其制备方法和用途
CN104597238B (zh) * 2015-01-27 2016-08-17 苏州博源医疗科技有限公司 一种霉酚酸均相酶免疫检测试剂及其制备和检测方法
CA3026241A1 (en) 2016-06-02 2017-12-07 Steven Baranowitz Prevention and treatment of viral infections
US12011429B2 (en) 2016-06-02 2024-06-18 Steven Baranowitz Prevention and treatment of viral infections
US10603299B2 (en) 2016-06-02 2020-03-31 Steven Baranowitz Prevention and treatment of viral infections
CN106674170B (zh) * 2016-12-30 2019-03-15 国家海洋局第三海洋研究所 三种苯酚类衍生物的制备方法及其在制备抗hiv药物中的应用

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US3825571A (en) * 1971-07-31 1974-07-23 Chugai Pharmaceutical Co Ltd Mycophenolic acid derivatives
JPS5542995B2 (es) * 1972-02-24 1980-11-04
JPS5529994B2 (es) * 1972-03-02 1980-08-07
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
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
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
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
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
CA2086642C (en) * 1992-01-09 2004-06-15 Randall E. Morris Method of treating hyperproliferative vascular disease
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
HRP950071A2 (en) 1997-06-30
PT745075E (pt) 2002-05-31
IL112667A (en) 2000-07-16
DE69524389D1 (de) 2002-01-17
SV1995000006A (es) 1996-09-30
JPH09509172A (ja) 1997-09-16
IS4265A (is) 1995-08-19
UY25263A1 (es) 2001-01-31
AU1917095A (en) 1995-09-04
DE69524389T2 (de) 2002-08-29
DK0745075T3 (da) 2002-03-04
TW369532B (en) 1999-09-11
UY23909A1 (es) 1995-03-06
PE23096A1 (es) 1996-06-04
EP0745075A1 (en) 1996-12-04
IL112667A0 (en) 1995-05-26
FI963221A (fi) 1996-10-16
FI963221A0 (fi) 1996-08-16
US5536747A (en) 1996-07-16
PH31406A (en) 1998-10-29
ES2168359T3 (es) 2002-06-16
CA2183533A1 (en) 1995-08-24
EP0745075B1 (en) 2001-12-05
MY130110A (en) 2007-06-29
US5444072A (en) 1995-08-22
BR9506835A (pt) 1997-10-14
HK1012634A1 (en) 1999-08-06
CN1141040A (zh) 1997-01-22
ZA951295B (en) 1996-08-16
WO1995022536A1 (en) 1995-08-24
SI0745075T1 (en) 2002-06-30
ATE210127T1 (de) 2001-12-15
GT199500006A (es) 1996-08-10

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