Agents for diagnosing and treating melanomas, aromatic halogenated derivatives usable as such agents and their preparation

• US 5,190,741 A
• Filed: 08/06/1991
• Issued: 03/02/1993
• Est. Priority Date: 02/14/1989
• Status: Expired due to Fees

• Current Assignee: Institut National De La Sante Et De La Recherche Medicale (Inserm) (Allianz Global Investors GmbH), CIS Bio International (Institut National Radio-Elements et D'Util Pub)
• Original Assignee: Institut National De La Sante Et De La Recherche Medicale (Inserm) (Allianz Global Investors GmbH), CIS Bio International (Institut National Radio-Elements et D'Util Pub)
• Inventors: Parry, Daniel, Lebarre, Pierre, Veyre, Annie J., Moreau, Marie-France, Meyniel, Gaston, Godeneche, Denise, Michelot, Josette, Madelmont, Jean-Claude
• Primary Examiner(s): Lovering, Richard D.
• Assistant Examiner(s): Sayala, C.
• Application Number:
  US07/741,481
• Time in Patent Office: 574 Days
• Field of Search: 424/1.1, 564/161
• US Class Current: 564/161
• CPC Class Codes: A61K 31/165 having aromatic rings, e.g. colchicine, atenolol, progabide
• CPC Class Codes: A61K 31/18 Sulfonamides compounds containing a para-N-benzene-sulfonyl-N- group A61K31/63
• CPC Class Codes: A61K 31/63 Compounds containing para-N-benzenesulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonyl hydrazide
• CPC Class Codes: A61K 51/0406 Amines, polyamines, e.g. spermine, spermidine, amino acids, (bis)guanidines
• CPC Class Codes: A61P 35/00 Antineoplastic agents
• CPC Class Codes: C07C 233/78 with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
• CPC Class Codes: C07C 311/18 to an acyclic carbon atom of a hydrocarbon radical substituted by nitrogen atoms, not being part of nitro or nitroso groups

Abstract

##STR1## The invention concerns agents for diagnosing and treating malignant melanomas, of general formula (I), in which X denotes a hydrogen or halogen atom, Y denotes a Z--CONH--, Z--O--, Z--S(O)--_n1 group, n₁ being equal to 0,1,2 or 3, a Z--SO₂ --NH-- Z--NHCO-- group, Z being a bond, a --CH₂ -- or --CH(C₆ H₅)-- group, n is an integer between 2 and 4, and R₁ and R₂ each denote a hydrogen atom, a C₁ to C₆ alkyl group or a C₆ to C₁₂ aryl or aralkyl group, these compounds possibly being labelled by radioisotopes chosen from ¹²³ I, ¹²³ I, ¹²³ I, ⁷⁵ Br, ⁷⁷ Br, ¹⁸ F, or ¹¹ C or by stable isotopes chosen from ¹³ C and ¹⁹ F, as well as their addition salts with pharmaceutically acceptable acids. The invention also concerns the use of these compounds to manufacture an agent for diagnosing and/or treating malignant melanomas.

Claims

1. A compound of formula ##STR12## wherein Y₁ represents a CO group,

I* represents ¹²⁵ I, ¹²³ I, ¹³¹ I

R₁ is selected from the group consisting of hydrogen, methyl, ethyl, propyl and isopropyl, and

R₂ is selected from the group consisting of hydrogen, methyl, ethyl, propyl and isopropyl.

2. A compound according to claim 1, which is ##STR13## *I being ¹²⁵ I, ¹²³ I or ¹³¹ I.