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US 2021/0230105 A1Published application
Compounds with biguanidyl radical and uses thereof
AssigneesInstitut Curie, lNSERM-INSTITUT NATIONAL DE LA SANTÉ ET DE LA RECHERCHE MÉDICALE, Centre National De La Recherche Scientifique
InventorsTATIANA CAÑEQUE, SEBASTIAN MULLER, RAPHAËL RODRIGUEZ
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Abstract
The present invention relates to new compounds of formula (I), and their uses.
Claims19
1-16. (canceled)
A compound of formula (I)
- wherein
- R1 is selected from the group consisting of a C1-C6 alkyl, —(CH2)a—C≡CH, —(CH2)b—P+Ph3, a C3-C10 cycloalkyl, a C3-C10 cycloheteroalkyl, a C6-C12 aryl, and a C5-C12 heteroaryl, with “a” being an integer selected from 1 to 6 and “b” being an integer selected from 5 to 11 said alkyl, cycloalkyl, cycloheteroalkyl, aryl or heteroaryl being optionally substituted by a R group or a R′ group;
- and
- R2 is selected from the group consisting of
- —(CH2)d—C≡CH, with “d” being an integer selected from 1 to 6;
- and
- —(CH2)e—CH═CH2 with “e” being an integer selected from 2 to 6;
- or
- R1 is selected from the group consisting of H, a C1-C6 alkyl, —(CH2)a—C≡CH, —(CH2)b—P+Ph3, a C3-C10 cycloalkyl, a C3-C10 cycloheteroalkyl, a C6-C12 aryl, and a C5-C12 heteroaryl, with “a” being an integer selected from 1 to 6 and “b” being an integer selected from 5 to 11, said alkyl, cycloalkyl, cycloheteroalkyl, aryl or heteroaryl being optionally substituted by a R group or a R′ group;
- R2 is selected from the group consisting of
- —(CH2)f-CR4═CH—CH═CR5—(CH2)g—R3 with R4 and R5 being H, a R group or forming together a six-member ring, optionally substituted by one or two R′ groups or fused with a cycloalkyl, an aryl, a cycloheteroalkyl or a heteroaryl having 3 to 6 members, “f” and “g” being an integer independently selected from 1 to 3;
- —(CH2)f—C≡C—C≡C—(CH2)g—R3, with “f” and “g” being an integer independently selected from 1 to 3;
- —(CH2)i—R3, with “i” being an integer selected from 7 to 9;
- —(CH2)j—CH[(CH2)k—P+Ph3]—(CH2)1—R3 with “j” and “1” being integer independently selected from 1 to 6, and “k” being an integer selected from 1 to 6;
- —(CH2)m-cyclobutanyl-(CH2)n—R3 with “m” and “n” being an integer independently selected from 1 to 3;
- and
- —(CH2)p—CHR6—CH═CH—CHR7—(CH2)q—R3 with R6 and R7 being H, a R group or forming together a 4-6 member ring, optionally substituted by one or two R′ groups or fused with a cycloalkyl, an aryl, a cycloheteroalkyl or a heteroaryl having 3 to 6 members, “p” and “q” being an integer independently selected from 1 to 3;
- and
- R3 is
- with R8 selected from the group consisting of H, a C1-C6 alkyl, —(CH2)a—C≡CH, —(CH2)b—P+Ph3, a C3-C10 cycloalkyl, a C3-C10 cycloheteroalkyl, a C6-C12 aryl, and a C5-C12 heteroaryl, with “a” being an integer selected from 1 to 6 and “b” being an integer selected from 5 to 11 said alkyl, cycloalkyl, cycloheteroalkyl, aryl or heteroaryl being optionally substituted by a R group or a R′ group;
- wherein
- R is selected from the group consisting of a C1-C6 alkyl, a C1-C6 alkyloxy, a C1-C6 halogenoalkyl, a C3-C10 cycloalkyl, a C3-C10 cycloheteroalkyl, a C6-C12 aryl, and a C5-C12 heteroaryl, the group being optionally substituted by a group R′,
- R′ is selected from the group consisting of a C1-C6 alkyl, a C1-C6 alkyloxy, a C1-C6 thioalkyl, a halogen, a C1-C6 halogenoalkyl, a hydroxyl (—OH), a cyano (—CN), a nitro, an amino (—NH2), a carboxyl (—COOH), a phosphate (PO4−), an amide (—CONH2), —COOR″, —NHR″, —NR″R′″, —COR″, —CONHR″, —NHCOR″, —NHSO2R″, —SOR″, —SO2R″, —SONR″R′″, —SO2NR″R′″, a C3-C10 cycloalkyl, a C3-C10 cycloheteroalkyl, a C6-C12 aryl, and a C5-C12 heteroaryl, said cycloalkyl, cycloheteroalkyl, aryl or heteroaryl being optionally substituted by a halogen, a hydroxyl, a cyano, a nitro, an amino, or a C1-C3 alkoxy, with R″ and R″' being H or a C1-C6 alkyl;
- or a pharmaceutically acceptable salt thereof.
21 more elements
Dependencies are inferred from the claim text.