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AP9400638A0 - Water soluble derivatives of camptothecin. - Google Patents

Water soluble derivatives of camptothecin.

Info

Publication number
AP9400638A0
AP9400638A0 APAP/P/1994/000638A AP9400638A AP9400638A0 AP 9400638 A0 AP9400638 A0 AP 9400638A0 AP 9400638 A AP9400638 A AP 9400638A AP 9400638 A0 AP9400638 A0 AP 9400638A0
Authority
AP
ARIPO
Prior art keywords
lower alkyl
amino
water soluble
methylpyrrolyl
furyl
Prior art date
Application number
APAP/P/1994/000638A
Inventor
Michael Joseph Luzzio
Jeffrey M Besterman
Michael Glenn Evans
Peter Leslie Myers
Original Assignee
Glaxo 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 Glaxo Inc filed Critical Glaxo Inc
Publication of AP9400638A0 publication Critical patent/AP9400638A0/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D317/00—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
    • C07D317/08—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3
    • C07D317/44—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D317/46—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C07D317/48—Methylenedioxybenzenes or hydrogenated methylenedioxybenzenes, unsubstituted on the hetero ring
    • C07D317/62—Methylenedioxybenzenes or hydrogenated methylenedioxybenzenes, unsubstituted on the hetero ring 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 atoms of the carbocyclic ring
    • C07D317/66—Nitrogen atoms not forming part of a nitro radical
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D319/00—Heterocyclic compounds containing six-membered rings having two oxygen atoms as the only ring hetero atoms
    • C07D319/10—1,4-Dioxanes; Hydrogenated 1,4-dioxanes
    • C07D319/14—1,4-Dioxanes; Hydrogenated 1,4-dioxanes condensed with carbocyclic rings or ring systems
    • C07D319/16—1,4-Dioxanes; Hydrogenated 1,4-dioxanes condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C07D319/18—Ethylenedioxybenzenes, not substituted on the hetero ring

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Compounds That Contain Two Or More Ring Oxygen Atoms (AREA)

Abstract

The present invention relates to water soluble, camptothecin derivatives of formula (1)wherein n represents the integer 1 or 2; and r1 represents hydrogen, lower alkyl, (c3-7)cycloalkyl, (c3-7)cycloalkyl lower alkyl, lower alkenyl, hydroxy lower alkyl, amino lower alkyl, lower alkylamino lower alkyl, amino lower alkul, lower alkoxy lower alkyl or (ch2)tar wherein: t is 0 to 5 and ar represents phenyl, furyl, pyridyl, n-methylpyrrolyl, imidazolyl; or phenyl, furyl, pyridyl, n-methylpyrrolyl, imidazolyl, with one or more substituents independtly selected from hydroxy, methoxy, halogen and amino; and r2 represents diphenylmenthyl or (ch2)tar; or r1 and r2 taken together with the linking nitrogen represents n-tetrahydroquinolyl or n-tetrahydroisoquinolyl; and pharmaceutically acceptable salts and solvents thereof; their use as topoisomerase inhibitors; their preparations; and their use in the treatment of cancer.
APAP/P/1994/000638A 1993-04-29 1994-04-28 Water soluble derivatives of camptothecin. AP9400638A0 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US5458593A 1993-04-29 1993-04-29
US8104293A 1993-06-22 1993-06-22

Publications (1)

Publication Number Publication Date
AP9400638A0 true AP9400638A0 (en) 1995-10-28

Family

ID=26733234

Family Applications (1)

Application Number Title Priority Date Filing Date
APAP/P/1994/000638A AP9400638A0 (en) 1993-04-29 1994-04-28 Water soluble derivatives of camptothecin.

Country Status (10)

Country Link
EP (1) EP0696285A1 (en)
JP (1) JPH08509740A (en)
AP (1) AP9400638A0 (en)
AU (1) AU6777194A (en)
CA (1) CA2161681A1 (en)
IL (1) IL109470A0 (en)
IS (1) IS4152A (en)
MY (1) MY141374A (en)
PE (1) PE52894A1 (en)
WO (1) WO1994025466A1 (en)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6504029B1 (en) * 1995-04-10 2003-01-07 Daiichi Pharmaceutical Co., Ltd. Condensed-hexacyclic compounds and a process therefor
US5663177A (en) * 1995-05-31 1997-09-02 Smithkline Beecham Corporation Water soluble camptothecin analogs
TW464652B (en) 1996-10-30 2001-11-21 Tanabe Seiyaku Co S type 2-substituted hydroxy-2-indolidinylbutyric ester compounds and process for preparation thereof
US6559309B2 (en) 1996-11-01 2003-05-06 Osi Pharmaceuticals, Inc. Preparation of a camptothecin derivative by intramolecular cyclisation
US6046209A (en) * 1997-05-27 2000-04-04 Smithkline Beecham Corporation Water soluble camptothecin analogs
IN189180B (en) * 1997-07-09 2003-01-04 Chong Kun Dang Corp
US6858598B1 (en) 1998-12-23 2005-02-22 G. D. Searle & Co. Method of using a matrix metalloproteinase inhibitor and one or more antineoplastic agents as a combination therapy in the treatment of neoplasia
US6833373B1 (en) 1998-12-23 2004-12-21 G.D. Searle & Co. Method of using an integrin antagonist and one or more antineoplastic agents as a combination therapy in the treatment of neoplasia
US6288072B1 (en) * 1999-12-29 2001-09-11 Monroe E. Wall Camptothecin β-alanine esters with topoisomerase I inhibition

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2165346T3 (en) * 1989-09-15 2002-03-16 Res Triangle Inst ANALOGS OF 10,11-METHYLENDIOXI-20 (RS) -CAMPTOTECINE AND 10.11-METHYLENDIOXI-20 (S) -CAMPTOTECINE.
EP0540099B1 (en) * 1991-10-29 1996-04-17 Glaxo Wellcome Inc. Water soluble camptothecin derivatives
EP0556585A3 (en) * 1992-01-24 1993-09-01 Takeda Chemical Industries, Ltd. Condensed camptothecin derivatives their production and use as antitumor agents

Also Published As

Publication number Publication date
AU6777194A (en) 1994-11-21
IL109470A0 (en) 1994-07-31
CA2161681A1 (en) 1994-11-10
IS4152A (en) 1994-10-30
WO1994025466A1 (en) 1994-11-10
EP0696285A1 (en) 1996-02-14
MY141374A (en) 2010-04-16
JPH08509740A (en) 1996-10-15
PE52894A1 (en) 1995-01-06

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