King Pharmaceuticals Research and Development, Inc.

Pharmacia & Upjohn

Università Degli Studi Di Ferrara

Katholieke Universiteit Leuven, Ku Leuven R&d

Universitá Degli Studi Di Padova

Pharmacia Italia S.p.a.

Associazione Veneta Per La Lotta Alla Talassemia

Associazione Per La Lotta Alla Talassemia Di Ferrara

Istituto Di Ricerca Pediatrica Citta Della Speranza

Katholieke Universiteit Leuven

King Pharmaceuticals, Inc.

Romeo Romagnoli

Pier Giovanni Baraldi

Italo Beria

Paolo Cozzi

Marina Caldarelli

Allan R Moorman

Laura Capolongo

Jan Balzarini

Maria Cristina Geroni

Roberto Gambari

Nicoletta Bianchi

Carlo Mischiati

Wim Dehaen

Giampiero Spalluto

Giordana Feriotto

Sandra Liekens

Joice Thomas

Giulia Pennella

Claudia Tregnago

Martina Pigazzi

The present invention relates to novel thioridazine analogue compounds of formula (I): wherein Ris OCHor NH, particularly suitable to be used in the treatment of pediatric acute myeloid leukemia harboring the t(6;11)(q27;q23) KMT2A/AFDN rearrangement.

Thioridazine derivatives and their use for the treatment of cancer

The present invention relates to compounds having cytostatic activity against tumor cells. The compounds of the invention are of formula (I), or derivatives hereof, wherein R, R, R, A, and X have defined meanings as described in claim. 

Anti-cancer compounds

The present invention provides compounds of formula (I) wherein R, R, R, Rand Q have a meaning as defined herein in the specification. The compounds of formula (I) are allosteric modulators of the Aadenosine receptor and, thus, may be employed for the treatment of conditions mediated by the Aadenosine receptor. Accordingly, the compounds of formula (I) may be employed for treatment of pain, in particular, chronic pain such as neuropathic pain; cardiac disease or disorder such as cardiac disarrhythmias, e.g., peroxysmal supraventricular tachycardia, angina, myocardial infarction and stroke; neurological disease or injury; sleep disorder; epilepsy; and depression.

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New fused thiophene compounds are provided and methods of using those compounds for a variety of therapeutic indications. Compounds of the invention are particularly useful for treatment of neuropathic pain.

Pharmaceutically active compounds and methods of use

The invention relates to the use of structural analogues of distamycin having the general formula (I), (II), (III), (IV) or (V) or their pharmaceutically acceptable salts, for the preparation of a medicament for the therapeutic treatment of &#x3b2;-thalassaemia.

Heterocyclic and benzoheterocyclic polyamides structurally related to the natural antibiotic distamycin A for the treatment of &#x3b2;-thalassaemia

Compounds which are acryloyl substituted distamycin derivatives of formula (I) wherein: n is 2, 3 or 4; m is 1 or 2; X and Y are the same or different and are selected, independently for each heterocyclic ring of the polyetherocyclic chain, from N and CH; R and R , which are the same or different, are selected from hydrogen, halogen, and C -C alkyl; R is hydrogen or halogen; B is selected from (a), (b), (c), (d), (e), (f), (g) and &mdash;C&equiv;N; wherein R , R , R , R , R , R , R , and R are, independently from each other, hydrogen or C -C alkyl; and R is hydrogen or hydroxy, or pharmaceutically acceptable salt thereof; provided that a) at least one of R , R and R is alkyl b) at least one of the heterocyclic rings within the polyheterocyclic chain is other than pyrole; and c) X and Y are not both N for the same heterocyclic ring; are useful as antitumor agents.

Acryloyl derivatives analogous to distamycin, process for preparing them, and their use as antitumor agents

Compounds which are cinnamoyl distamycin derivatives of formula (I), wherein n is 2, 3, or 4; R is C -C alkyl or C -C haloalkyl; R and R , which are the same or different, are selected from hydrogen, C -C alkyl optionally substituted by one or more fluorine atoms; and C -C alkoxy; X is a halogen atom; Y and Z are the same or different and are selected, independently for each heterocyclic ring of the polyheterocyclic chain, from N and CH; B is selected from (a), (b), (c), (d), (e), (f), (g)and (h) wherein R , R , R , R and R are, independently from each other, hydrogen or C -C alkyl; or pharmaceutically acceptable salts thereof; provided that at least one of the heterocyclic rings within the polyheterocyclic chain is other than pyrrole; are useful as antitumor agents.

Cinnamoyl distamycin analogous derivatives, process for their preparation, and their use as antitumor agents

Compounds which are benzoheterocyclic distamycin derivatives of formula (I), wherein n is 2, 3 or 4; A is a heteroatom selected from O and S or is a group NR, wherein R is hydrogen or C -C alkyl; B is CH or N; R is hydrogen or C -C alkyl; G is selected from the group consisting of (a, b, c, d, e, f, g, h, i, j), and &mdash;C&equiv;N; wherein R , R , R , R , R , R , R and R are, independently from each other, hydrogen or C -C alkyl; T is a group of formula (II) or (III) as defined above, wherein p is 0 or 1; R and R are, independently from each other, hydrogen, C -C alkyl optionally substituted by one or more fluorine atoms, or C -C alkoxy; R is C -C alkyl or C -C haloalkyl; X and X are halogen atoms or pharmaceutically acceptable salts thereof; provided that at least one of R , R and R is alkyl; are useful as antitumor agents.

Benzoheterocyclic distamycin derivatives, process for preparing them, and their use as antitumor agents

Benzoheterocyclic distamycin derivatives, process for preparing them,

Growing community of inventors

Ferrara, Italy

Romeo Romagnoli