King Pharmaceuticals Research and Development, Inc.

Pharmeste S.r.l.

Medco Research, Inc.

King Pharmacueticals Reserch and Development, Inc.

King Pharmaceuticuals Research & Development, Inc.

King Pharmaceuticals Reseach and Development, Inc.

Università Degli Studi Di Firenze

Università Degli Studi Di Ferrara

Pier Andrea Borea

Pier Giovanni Baraldi

Pierangelo Geppetti

Allan R Moorman

Maria Giovanna Pavani

Francesca Fruttarolo

Marcello Trevisani

Mojgan Aghazadeh Tabrizi

Delia Preti

Edward Leung

Shih-Fong Chen

Fabrizio Vincenzi

Daniela Catarzi

Katia Varani

Vittoria Colotta

Flavia Varano

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 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.

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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

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 present invention relates generally to compounds of formula (I): wherein The present invention also relates to the preparation of the compounds, pharmaceutical formulations thereof, and their use in medicine as potent or selective Aadenosine receptor antagonists and their uses for treating asthma, autoimmune diseases and retinal vascular diseases.

The present invention relates generally to compounds of the formula (I): wherein:

The present invention relates to compounds of the formula 

Tyrosyl derivatives and their use as P2X7 receptor modulators

New compounds having a tricyclic pyrazolotriazolopyrimidine ring structure are provided and methods of using those compounds for a variety of therapeutic indications.

Growing community of inventors

Ferrara, Italy

Pier Andrea Borea