Radioactive iodine labeled pyrido[1,2-a]benzoimidazole derivative compound

Patent metadata

Field	Value
Publication number	US-10080812-B2
Application number	US-201615543857-A
Country	US
Kind code	B2
Filing date	Feb 24, 2016
Priority date	Mar 4, 2015
Publication date	Sep 25, 2018
Grant date	Sep 25, 2018

Abstract

The present invention relates to a radioactive iodine-labeled pyrido[1,2-a]benzimidazole derivative compound represented by a definite general formula or a salt thereof, or a radiopharmaceutical comprising the same.

First claim

The invention claimed is:

1. A radioactive iodine-labeled compound represented by the following formula (1) or a salt thereof:

wherein when R 1 is a hydrogen atom, R 2 is a radioactive iodine atom or a radioactive iodophenyl group, and when R 1 is a radioactive iodine atom, R 2 is a hydrogen atom or a phenyl group.

2. The radioactive iodine-labeled compound or a salt thereof according to claim 1 , wherein the radioactive iodophenyl group is a substituent having a phenyl group which hydrogen atom at position 4 is substituted with a radioactive iodine atom.

3. The radioactive iodine-labeled compound or a salt thereof according to claim 1 , wherein the radioactive iodine atom is 123 I, 124 I, 125 I, or 131 I.

4. A radiopharmaceutical comprising a radioactive iodine-labeled compound or a salt thereof according to claim 1 .

5. The radiopharmaceutical according to claim 4 , which is for use in single photon emission computed tomography (SPECT).

6. A diagnostic agent for Alzheimer's disease comprising a radioactive iodine-labeled compound or a salt thereof according to claim 1 .

7. A compound represented by the following formula (2) or a salt thereof:

wherein when R 3 is a hydrogen atom, R 4 is a trialkylstannyl group, a trialkylsilyl group, a trialkylstannyl phenyl group, or a trialkylsilyl phenyl group, and when R 3 is a trialkylstannyl group or a trialkylsilyl group, R 4 is a hydrogen atom or a phenyl group.

8. A method for producing a radioactive iodine-labeled compound, comprising the step of sublectinq a compound represented by the following formula (2) or a salt thereof to a radioactive iodination reaction to obtain a radioactive iodine-labeled compound represented by the following formula (1):

wherein when R 3 is a hydrogen atom, R 4 is a trialkylstannyl group, a trialkylsilyl group, a trialkylstannyl phenyl group, or a trialkylsilyl phenyl group, and when R 3 is a trialkylstannyl group or a trialkylsilyl group, R 4 is a hydrogen atom or a phenyl group, and

wherein when R 1 is a hydrogen atom, R 2 is a radioactive iodine atom or a radioactive iodophenyl group, and when R 1 is a radioactive iodine atom, R 2 is a hydrogen atom or a phenyl group.

Assignees

• Univ Kyoto
• Nihon Mediphysics Co Ltd

Inventors

• Saji Hideo
• Ono Masahiro
• Ihara Masafumi
• Seki Ikuya

Classifications

• A61P25/28

  for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia · CPC title

• C07F7/10

  containing nitrogen {having a Si-N linkage} · CPC title

• C07B59/00 Primary

  Introduction of isotopes of elements into organic compounds {; Labelled organic compounds per se} · CPC title

• C07F7/22

  Tin compounds · CPC title

• C07F7/0814

  said ring is substituted at a C ring atom by Si · CPC title