COMPOUND HAVING TUMOR-RESIDENT PROPERTY

• US 20100202971A1
• Filed: 01/15/2010
• Published: 08/12/2010
• Est. Priority Date: 01/16/2009
• Status: Abandoned Application

• Current Assignee: Fumio Sugawara, Hiroshi Murata, Keisuke Ohta, Kengo Sakaguchi, Masahiko Miura, Masahiro Ishima
• Original Assignee: Fumio Sugawara, Hiroshi Murata, Keisuke Ohta, Kengo Sakaguchi, Masahiko Miura, Masahiro Ishima
• Inventors: Ishima, Masahiro, OHTA, Keisuke, Murata, Hiroshi, Sugawara, Fumio, Sakaguchi, Kengo, Miura, Masahiko
• Application Number:
  US12/688,153
• Publication Number:
  US 20100202971A1
• Time in Patent Office: Days
• US Class Current: 424/9.100
• CPC Class Codes: A61K 47/551 one of the codrug's components being a vitamin, e.g. niacinamide, vitamin B3, cobalamin, vitamin B12, folate, vitamin A or retinoic acid
• CPC Class Codes: A61P 35/00 Antineoplastic agents
• CPC Class Codes: C07H 15/04 attached to an oxygen atom of the saccharide radical
• CPC Class Codes: C07H 15/06 being a hydroxyalkyl group esterified by a fatty acid
• CPC Class Codes: C07H 15/08 Polyoxyalkylene derivatives
• CPC Class Codes: C07H 15/10 containing unsaturated carbon-to-carbon bonds
• CPC Class Codes: C07H 15/18 Acyclic radicals, substituted by carbocyclic rings

Abstract

The problem to be solved of the present invention is to provide a novel compound which specifically resides in a tumor, a method for allowing it to reside in a tumor, and a method for detecting, diagnosing, and treating tumor with use thereof. Means for solving the problem is a compound represented by chemical formula (I)

wherein R is an anionic group binding to hydrogen, R₁ is OH, OCOH, OCO(CH₂)_hCH₃, or an acting group, h being an integer of 0 or more, R₂ is H, OH, OCOH, OCO(CH₂)_iCH₃, or an acting group, i being an integer of 0 or more, R₃ is OH, SO₃H, or an acting group, R₄ is OH, SO₃H, or an acting group, and R₅ is OH, SO₃H, or an acting group, at least one of R₁, R₂, R₃, R₄, and R₅ containing an acting group, or pharmaceutically acceptable salts thereof.

Claims

1. A compound represented by chemical formula (I):

3. The compound or salts according to claim 1 or 2,

wherein R is SO₃H,

R₃ is OH,

R₄ is OH,

R₅ is OH,

R₁ is OH, OCOH, OCO(CH₂)_hCH₃, O—

(an acting group), OCO—

(an acting group), or OCO(CH₂)_hCH₂—

(an acting group), h being an integer of 0 or more, and

R₂ is H, OH, OCOH, OCO(CH₂)_iCH₃, an acting group, O—

(an acting group), OCO—

(an acting group), or OCO(CH₂)_iCH₂—

(an acting group), i being an integer of 0 or more,

at least one of R₁ and R₂ containing an acting group.

4. The compound or salts according to claim 1 or 2,

wherein R is SO₃H,

R₁ is OH, OCOH, OCO(CH₂)_hCH₃, or an acting group, h being an integer of 0 or more,

R₂ is H, OH, OCOH, OCO(CH₂)_iCH₃ or an acting group, i being an integer of 0 or more, and

R₃═

R₄═

R₅ is OH, or at least one of R₃, R₄ and R₅ contains an acting group and the other groups are OH,

at least one of R₁, R₂, R₃, R₄, and R₅ containing an acting group.

6. The compound or salts according to any one of claims 1-5, wherein the acting group is a labeled substance or an antitumor substance.

7. A method for allowing the compound represented by formula (I) or (II) or salts to reside in a tumor, wherein the compound or salts according to any one of claims 1-6 are administered to a subject.

8. A method for detecting tumor, comprising:

administering the compound or salts according to any one of claims 1-5 to a subject, wherein the acting group is a labeled substance;

detecting the labeled substance when the compound or salts exist in a higher concentration in a tumor than in other tissues except a tumor; and

detecting tumor in the subject based on results of the detecting.

9. A method for diagnosing tumor, comprising:

administering the compound or salts according to any one of claims 1-5 to a subject, wherein the acting group is a labeled substance;

detecting the labeled substance when the compound or salts exist in a higher concentration in a tumor than in other tissues except a tumor; and

determining presence or absence of tumor in the subject based on results of the detecting.

10. A method according to claim 8 or 9, wherein the detecting is carried out by a noninvasive means.

11. A method for treating tumor, comprising administering the compound or salts according to any one of claims 1-5 to a subject, wherein the acting group is an antitumor substance.

2. A compound represented by chemical formula (II):

5. Sulfopyranosyl(acyl)glycerol, sulfopyranosyl(acyl)propanediol, or sulfoquinovosylacyl propanediol, wherein any of side residues binds to an acting group,

or pharmaceutically acceptable salts.