CA2219659A1 - Rapamycin derivatives - Google Patents

Rapamycin derivatives

Info

Publication number
CA2219659A1
CA2219659A1 CA002219659A CA2219659A CA2219659A1 CA 2219659 A1 CA2219659 A1 CA 2219659A1 CA 002219659 A CA002219659 A CA 002219659A CA 2219659 A CA2219659 A CA 2219659A CA 2219659 A1 CA2219659 A1 CA 2219659A1
Authority
CA
Canada
Prior art keywords
rapamycin derivatives
formula
rapamycin
derivatives
iii
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.)
Granted
Application number
CA002219659A
Other languages
French (fr)
Other versions
CA2219659C (en
Inventor
Sylvain Cottens
Richard Sedrani
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.)
Novartis AG
Original Assignee
Individual
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
Priority claimed from GBGB9511704.0A external-priority patent/GB9511704D0/en
Priority claimed from GBGB9513754.3A external-priority patent/GB9513754D0/en
Application filed by Individual filed Critical Individual
Publication of CA2219659A1 publication Critical patent/CA2219659A1/en
Application granted granted Critical
Publication of CA2219659C publication Critical patent/CA2219659C/en
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/18—Bridged systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic System
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
    • C07F7/1804—Compounds having Si-O-C linkages

Abstract

Compounds of Formula (I), wherein R2 is selected from formula (II) or formula (III), and X is OH or H show immunosuppressant activity.
CA002219659A 1995-06-09 1996-06-05 Rapamycin derivatives Expired - Lifetime CA2219659C (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
GB9511704.0 1995-06-09
GBGB9511704.0A GB9511704D0 (en) 1995-06-09 1995-06-09 Organic compounds
GB9513754.3 1995-07-06
GBGB9513754.3A GB9513754D0 (en) 1995-07-06 1995-07-06 Organic compounds
PCT/EP1996/002441 WO1996041807A1 (en) 1995-06-09 1996-06-05 Rapamycin derivatives

Publications (2)

Publication Number Publication Date
CA2219659A1 true CA2219659A1 (en) 1996-12-27
CA2219659C CA2219659C (en) 2008-03-18

Family

ID=26307190

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002219659A Expired - Lifetime CA2219659C (en) 1995-06-09 1996-06-05 Rapamycin derivatives

Country Status (30)

Country Link
US (2) US5985890A (en)
EP (1) EP0833828B1 (en)
JP (1) JP3226545B2 (en)
KR (1) KR100400620B1 (en)
CN (1) CN1124276C (en)
AR (1) AR003426A1 (en)
AT (1) ATE228135T1 (en)
AU (1) AU712193B2 (en)
BR (1) BR9609260A (en)
CA (1) CA2219659C (en)
CO (1) CO4440629A1 (en)
CZ (1) CZ292233B6 (en)
DE (1) DE69624921T2 (en)
DK (1) DK0833828T3 (en)
ES (1) ES2187660T3 (en)
FI (1) FI113051B (en)
HK (1) HK1014949A1 (en)
HU (1) HU228234B1 (en)
IL (1) IL122212A (en)
MY (1) MY145291A (en)
NO (1) NO317058B1 (en)
NZ (1) NZ311647A (en)
PE (1) PE4598A1 (en)
PL (1) PL184731B1 (en)
PT (1) PT833828E (en)
RU (1) RU2158267C2 (en)
SK (1) SK284529B6 (en)
TR (1) TR199701567T1 (en)
TW (1) TW410226B (en)
WO (1) WO1996041807A1 (en)

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