King Pharmaceuticals Research and Development, Inc.

Pharmeste S.r.l.

Medco Research, Inc.

Pharmacia & Upjohn

The University of Ferrara

Medco, LLC

Schering Corporation

Katholieke Universiteit Leuven

Pharmacia Corporation

Pharmacia Italia S.p.a.

Associazione Veneta Per La Lotta Alla Talassemia

Associazione Per La Lotta Alla Talassemia Di Ferrara

King Pharmaceutical Research & Development, Inc.

King Pharmacueticals Reserch and Development, Inc.

King Pharmaceuticals, Inc.

Pier Giovanni Baraldi

Pier Andrea Borea

Romeo Romagnoli

Allan R Moorman

Italo Beria

Pierangelo Geppetti

Paolo Cozzi

Marina Caldarelli

Laura Capolongo

Maria Giovanna Pavani

Francesca Fruttarolo

Marcello Trevisani

Mojgan Aghazadeh Tabrizi

Delia Preti

Jan Balzarini

Ennio Ongini

Nicola Mongelli

Enrico Pesenti

Roberto Gambari

Maria Cristina Geroni

Edward Leung

Nicoletta Bianchi

Wim Dehaen

Carlo Mischiati

Giampiero Spalluto

Giordana Feriotto

Joice Thomas

Sandra Liekens

Giulia Pennella

Shih-Fong Chen

Silvio Dionisotti

Monica Valeria Viziano

Barbara Cacciari

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 A and Z are as defined in the description, along with methods for preparing such derivatives and their use for the treatment of inflammatory diseases such as neuropathic pain. 

Biarylcarboxyarylamides as vanilloid-1 receptor modulators

The invention relates to compounds of formula (I), wherein R, R, R, X and n are as defined in the description, and their use for the preparation of pharmaceutical compositions for the treatment of inflammatory states.

Vanilloid TRPV1 receptor antagonists

The invention provides compounds of formula (I), wherein Y, R, n and X are as defined in the description, a process for their preparation and pharmaceutical compositions containing them. The compounds of formula (I) inhibit the Transient Receptor Potential Vanilloid 1 (TRPV1), which plays a pivotal role in the development of post-inflammatory analgesia, therefore they can be used as analgesic and anti-inflammatory drugs. 

VR1 vanilloid receptor antagonists with a iononic substructure

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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The present invention provides compounds of the formula which are adenosine Areceptor antagonists and, thus, may be employed for the treatment of conditions and diseases mediated by the adenosine Areceptor activity. Such conditions include, but are not limited to, chronic and acute inflammatory diseases involving degranulation of mast cells, e.g., asthma, allergic rhinitis and allergic dermatitis; impaired sensitivity to insulin, e.g., type 2 diabetes, pre-diabetic state, and impaired glucose tolerance; diseases in which angiogenesis is a key component of pathogenesis, e.g., solid tumors and angiogenic retinopathies; apnea of preterm infants; myocardial reperfusion injury; inflammatory bowel disease; autoimmune diseases, such as rheumatoid arthritis, multiple sclerosis, and lupus erythematosis; diseases involving microvascular abnormalities of the retina that are mediated by adenosine Areceptors, e.g., retinopathy of prematurity, macular degeneration, and diabetic retinopathy; and cardiac diseases including hyperplasia consequent to hypertension, arteriosclerosis, and heart attack.

Adenosine A2B receptor antagonists

The invention relates to compounds of formula (I) in which R is selected from halogen, alkyl, alkoxy, aryl and heteroaryl; Ris selected from 2-hydroxyethyl, 2,3-dihydroxypropyl, 3-hydroxypropyl, 2,2-dihydroxyethyl, 3,3-dihydroxypropyl, 1,3-dioxolane-ethyl, 1,3-dioxane-methyl, 1,3-dioxolane-methyl, 1,3-dioxane-ethyl, 3-fluoro-2-hydroxypropyl, 3-carboxy-2-hydroxy-propyl, 3-chloro-2-hydroxypropyl, 2-hydroxypropyl, 2-hydroxy-propen-2-yl, morpholinoethyl, piperazinoethyl, hydroxymethyl, benzyl, 4-(hydroxymethyl)benzyl, 4-chlorobenzyl, 4-fluorobenzyl, and 4-hydroxybenzyl. Ris te/t-butyl or trifluoromethyl; R3 is independently selected from hydrogen, carboxy, cyano, alkyl or hydroxyalkyl, The compounds of formula (I) can be used for the preparation of pharmaceutical compositions for the therapy of inflammatory states, such as chronic neuropathic pain, over-active bladder syndrome, tumor pain, hemorrhoids, inflammatory hyperalgesia, post-intervention pain, dental extraction, airway and gastro-intestinal diseases. 

O-substituted-dibenzyl urea-derivatives as TRPV1 receptor antagonists

The present invention provides compounds of the formula wherein R, R, Rand n have meaning as described in the specification, methods for their preparation, and pharmaceutical compositions containing them. The compounds of formula (I) are adenosine Areceptor agonists and, thus, may be employed for the treatment of diseases in mammals that are mediated by the Areceptor including, but not limited to, septic shock, cystic fibrosis, impotence, diarrhea, and cardiac diseases. Cardiac diseases include hyperplasia consequent to hypertension, arteriosclerosis, and heart attack. The present invention also provides methods for the induction of pharmacological stress to facilitate coronary imaging of areas of ischemia by employing compounds of formula (I). The compounds of formula (I) may be labeled, e.g., with radioactive isotopes, and therefore are useful in kinetic binding experiments.

The invention relates to sulfonamido derivatives of formula (I) wherein R-Rare as defined in the description. Compounds (I) antagonize the vanilloid receptor and can be used for the preparation of medicaments for the treatment of inflammatory states.

Sulfonamido compounds that antagonize the vanilloid TRPV1 receptor

The compounds of the following formula: wherein R, R, Rand A have the meanings given in the specification, are endowed with selective Aadenosine receptor antagonist activity. These compounds can be used in a pharmaceutical composition to treat disorders caused by excessive activation of the Areceptor, or can be used in a diagnostic application to determine the relative binding of other compounds to the Areceptor. The compounds can be labeled, for example with fluorescent or radiolabels, and the labels used in vivo or in vitro to determine the presence of tumor cells which possess a high concentration of adenosine Areceptors.

Adenosine A3 receptor modulators

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

A class of novel antagonists for the adenosine Areceptor are disclosed. These compounds are useful as therapeutic agents for a number of diseases and medical conditions that are mediated by the Areceptor. The compounds of this invention are also useful as diagnostic agents for the Areceptor.

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

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Ferrara, Italy

Pier Giovanni Baraldi