The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.
The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.
Patent No.:
Date of Patent:
Feb. 07, 2017
Filed:
Mar. 28, 2013
Nerviano Medical Sciences S.r.l., Nerviano, IT;
Italo Beria, Nerviano, IT;
Michele Caruso, Milan, IT;
Vittoria Lupi, Milan, IT;
Paolo Orsini, Legnano, IT;
Matteo Salsa, Bellinzago Novarese, IT;
NERVIANO MEDICAL SCIENCES S.R.L., Nerviano (MI), IT;
Abstract
The invention relates to new functionalized thieno-indole derivatives of formula (I) or (II) which have cytotoxic activity and are useful in treating diseases such as cancer and cellular proliferation disorders. The invention also relates to the use of these functionalized thieno-indole derivatives in the preparation of conjugates. Formula (I) or (II) wherein Rand Rtaken together form a group (D) or (G): wherein Ris hydrogen or C-Calkyl; Rand Rare independently hydrogen, C-Calkyl or C-Chydroxyalkyl; n is 0, 1 or 2; each of X is independently —O—, —S— or —NR—; each of Y is independently —CH═ or —N═; Rand Rare independently hydrogen, halogen, hydroxy, C-Calkoxy, cyano, —NHCOOR, —C(NH)NHor —NRR; A is —O—, —NH— or —CO—; L is null or a conditionally-cleavable moiety; W is null or a self-immolative moiety comprising one or more self-immolative groups; Z is null or a peptidic, non peptidic or hybrid peptidic and non peptidic linker; RM is null or a reactive moiety; Ris a leaving group; Ais null or A; Lis hydrogen or L.