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EP0470569B1 Expired / Lapsed EP ⏱️ 0.0 years remaining

Intravascular embolizing agent containing angiogenesis inhibiting substance

Assignee: Takeda Pharmaceutical Co Ltd
•
Filing: 1991-08-06
•
Granted: 1995-11-22
•
Expires: 2011-08-06
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Abstract

Abstract The present invention relates to an intravascular embolizing agent containing an angiogenesis-inhibiting substance and an intravascular embolizing substance. The agent strengthens the antitumor effect of an angiogenesis-inhibiting substance and serves to reduce the dose and undesirable side effects. And use of the agent in concert with an anti-neoplastic agent brings about further strong and long-lasting antitumor effects.

Inventors

  • 👤 Hiroaki Okada
  • 👤 Shigeru Kamei
  • 👤 Toshio Yoshioka

Bibliographic Details

Application Number —
Jurisdiction EP
Data Source google_patents
Last Synchronized 2026-10-25 23:23
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/70; A61K31/715; A61K31/74; A61K31/765; A61K38/00; A61K38/16; A61K38/17; A61K38/38; A61K38/39; A61K9/00; A61K9/14; A61K9/16; A61K9/1605; A61K9/1629; A61K9/1641; A61K9/1647; A61K9/1658; A61P; A61P35/00; A61P9/00; A61P9/14

Claims Analysis

Total Claims: 20
Claim 1
Independent Claim 208 words
A process for preparing an intravascular embolizing agent containing an angiogenesis-inhibiting substance and an intravascular embolizing substance which process is selected from a) when intravascular embolizing substance and angiogenesis inhibiting substance are soluble in an organic solvent, dissolving both substances in an organic solvent, followed by dispersing in an aqueous phase containing a surfactant or a protective colloid, or by spray-drying to evaporate of the organic solvent; b) when the intravascular embolizing substance is soluble in an organic solvent and the angiogenesis inhibiting substance is water-soluble, dispersing an aqueous solution of the angiogenesis inhibiting substance in a solution of the intravascular embolizing substance in an organic solvent, followed by evaporating of the organic solvent; c) when the intravascular embolizing substance is water-soluble and the angiogenesis inhibiting substance is soluble in an organic solvent, dispersing the angiogenesis inhibiting substance in an aqueous solution of the intravascular embolizing substance, or dissolving the angiogenesis inhibiting substance in a volatile organic solvent, dispersing said solution in an aqueous solution of the intravascular embolizing substance, dispersing the above prepared liquid preparation in an oily phase, followed by solidification; and d) when intravascular embolizing substance and angiogenesis inhibiting substance are water-soluble, dissolving both substances in water, dispersing in an oily phase, followed by solidification.
Claim 2
Dependent Claim 26 words
A process as claimed in Claim 1 wherein the prepared intravascular embolizing agent is in the state of an oil solution, an emulsion or a suspension.
Claim 3
Dependent Claim 32 words
A process as claimed in Claim 1 wherein the prepared intravascular embolizing agent is in the state of an emulsion or suspension containing granules whose size ranges from 10 to 1000 µm.
Claim 4
Dependent Claim 15 words
A process as claimed in Claim 1 wherein the angiogenesis-inhibiting substance is a fumagillol derivative.
Claim 5
Dependent Claim 13 words
A process as claimed in Claim 1 wherein the angiogenesis-inhibiting substance is 6-O-(N-chloroacetylcarbamoyl)fumagillol.
Claim 6
Dependent Claim 14 words
A process as claimed in Claim 1 wherein the angiogenesis-inhibiting substance is 6α-(N'-chloroacetylureido)-6-desoxy fumagillol.
Claim 7
Dependent Claim 14 words
A process as claimed in Claim 1 wherein the angiogenesis-inhibiting substance is 4-(N'-chloroacetyluredio)-2-(1,2-epoxy-1,5-dimethyl-4-hexenyl)-1-(1,3-dihydrobenzo[c]thiophene-2-ylio)methyl-3-methoxycyclohexanol chloride.
Claim 8
Dependent Claim 24 words
A process as claimed in Claim 1 wherein the prepared intravascular embolizing agent is having the angiogenesis-inhibiting substance included in the intravascular embolizing substance.
Claim 9
Dependent Claim 26 words
A process as claimed in Claim 1 characterized in that in the prepared intravascular embolizing agent the angiogenesis-inhibiting substance is adsorbed on the intravascular embolizing substance.
Claim 10
Dependent Claim 41 words
A process as claimed in Claim 1 wherein the intravascular embolizing substance is an oil, a metal, an insoluble salt of metal, a ceramic, wax, activated carbon, polypeptide, polysaccharide, hydroxycarboxylic acid polymer, polyamino acid, polyaldehyde, polyvinyl polymer or maleic anhydride polymer.
Claim 11
Dependent Claim 24 words
A process as claimed in Claim 1 wherein the intravascular embolizing substance is a polymer which gradually dissolves or decomposes in a living body.
Claim 12
Dependent Claim 24 words
A process as claimed in Claim 1 wherein the intravascular embolizing substance is gelatin, albumin, collagen, starch hyaluronic acid or lactic acid-glycolic acid copolymer.
Claim 13
Dependent Claim 43 words
A process as claimed in Claim 1 wherein the intravascular embolizing substance is a lactic acid-glycolic acid copolymer whose molar ratio of lactic acid and glycolic acid is in the range of 100/1 to 30/70 and molecular weight ranges from 1,000 to 100,000.
Claim 14
Dependent Claim 26 words
A process as claimed in Claim 1 wherein the angiogenesis-inhibiting substance is a fumagillol derivative and the intravascular embolizing substance is a lactic acid-glycolic acid copolymer.
Claim 15
Dependent Claim 24 words
A process as claimed in Claim 1 wherein the angiogenesis-inhibiting substance is 6-O-(N-chloroacetylcarbamoyl)fumagillol and the intravascular embolizing substance is a lactic acid-glycolic acid copolymer.
Claim 16
Dependent Claim 25 words
A process as claimed in Claim 1 wherein the angiogenesis-inhibiting substance is 6α-(N'-chloroacetylureido)-6-desoxy fumagillol and the intravascular embolizing substance is a lactic acid-glycolic acid copolymer.
Claim 17
Dependent Claim 24 words
A process as claimed in Claim 1 wherein the angiogenesis-inhibiting substance is 4-(N'-chloroacetyluredio)-2-(1,2-epoxy-1,5-dimethyl-4-hexenyl)-1-(1,3-dihydrobenzo[c]thiophene-2-ylio)methyl-3-methoxycyclohexanol chloride and the intravascular embolizing substance is lactic acid-glycolic acid copolymer.
Claim 18
Dependent Claim 20 words
A process as claimed in claim 1 characterized in that the prepared intravascular embolizing agent further contains an anti-neoplastic agent.
Claim 19
Dependent Claim 19 words
A process according to any of claims 1-18 wherein the intravascular embolizing agent further comprises a pharmaceutically acceptable carrier.
Claim 20
Dependent Claim 23 words
Use of an intravascular embolizing agent as claimed in Claim 1 for the preparation of a pharmaceutically acceptable composition for treatment of cancer.

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