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US 2019/0337916 A1Published application
Notch inhibitors for use in the treatment of t-cell acute lymphoblastic leukemia
AssigneesUniversita' Degli Studi Di Roma “La Sapienza”, Fondazione Istituto Italiano Di Tecnologia
InventorsBruno Botta, Isabella Screpanti, Luca Tottone, Nadezda Zhdanoskaya, Cinzia Ingallina, Francesca Giulimondi, Deborah Quaglio, Rocco Palermo, Mattia Mori, Francesca Ghirga
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Abstract
Compounds of formula (I) in the capacity of compounds with anti-tumor activity for the treatment of T-cell acute lymphoblastic leukemia (T-ALL).
Claims10
A method of treating T-cell acute lymphoblastic leukemia (T-ALL) in a subject, comprising administering to the subject a compound of formula (I),
- wherein
- X and Y are carbon atoms bound by a single or double bond having, independently, an E or Z configuration;
- R1′ is hydrogen, halogen, ORA, C(═O)RA, C(═O)ORA, OC(═O)RA, SRA, SO2RA, SO3RA, OSO2RA, OSO3RA, N(RA)2, NHC(═O)RA, C(═O)N(RA)2, or C(RA)3;
- R2′, R3′, R1, R2, R3 are the same or different and independently selected from:
- hydrogen;
- halogen;
- ORB;
- C(═O)RB;
- C(═O)ORB;
- OC(═O)RB;
- SRB;
- SO2RB;
- SO3RB;
- OSO2RB;
- OSO3RB;
- N(RB)2;
- NHC(═O)RB;
- C(═O)N(RB)2;
- C(RB)3;
- a linear or branched, saturated or unsaturated C1-7 acyclic aliphatic group optionally containing up to three heteroatoms independently selected from nitrogen, oxygen or sulfur;
- a C5-7 cycloalkyl group;
- a phenyl;
- a C5-7 heterocyclic group;
- wherein at each occurrence RA and RB are independently selected from:
- hydrogen;
- a linear or branched, saturated or unsaturated C1-7 aliphatic group optionally containing up to three heteroatoms independently selected from nitrogen, oxygen or sulfur;
- a C5-7 cycloalkyl group;
- a phenyl group;
- a C5-7 heterocyclic group;
- and pharmaceutically acceptable salts thereof.
27 more elements
A compound of formula (I)
- wherein
- X and Y are carbon atoms bound by a single or double bond having, independently, an E or Z configuration;
- R1′ is hydrogen, halogen, ORA, C(═O)RA, C(═O)ORA, OC(═O)RASRA, SO2RA, SO3RA, OSO2RA, OSO3RA, N(RA)2, NHC(═O)RA, C(═O)N(RA)2, or C(RA)3;
- R2′, R3′, R1, R2, R3 are the same or different and independently selected from:
- hydrogen;
- halogen;
- ORB;
- C(═O)RB;
- C(═O)ORB;
- OC(═O)RB;
- SRB;
- SO2RB;
- SO3RB;
- OSO2RB;
- OSO3RB;
- N(RB)2;
- NHC(═O)RB;
- C(═O)N(RB)2;
- C(RB)3;
- a linear or branched, saturated or unsaturated C1-7 acyclic aliphatic group optionally containing up to three heteroatoms independently selected from nitrogen, oxygen or sulfur;
- a C5-7 cycloalkyl group;
- a phenyl;
- a C5-7 heterocyclic group;
- wherein at each occurrence RA and RB are independently selected from:
- hydrogen;
- a linear or branched, saturated or unsaturated C1-7 aliphatic group optionally containing up to three heteroatoms independently selected from nitrogen, oxygen or sulfur;
- a C5-7 cycloalkyl group;
- a phenyl group;
- a C5-7 heterocyclic group;
- and salts thereof,
- with the provision that the compound of formula (I) is not 2′,3,4,4′-tetramethoxychalcone or 2′,4,4′-trimethoxychalcone.
28 more elements
Dependencies are inferred from the claim text.