Patents by Inventor Pier Andrea Borea
Pier Andrea Borea has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).
-
Publication number: 20200308192Abstract: The present invention refers to novel thiazolo[5,4-d]pyrimidine derivatives that are inverse agonists of the adenosine A2A receptor, to a process for their preparation, to the pharmaceutical compositions containing them and to their use in the medical field, in particular in the therapeutic treatment of diseases or disorders associated to an activity of the adenosine A2A receptor, and more in particular in the therapeutic treatment of neurological diseases, of pain, of cancer, and of dermal fibrosis and scarring.Type: ApplicationFiled: July 5, 2017Publication date: October 1, 2020Inventors: Flavia VARANO, Vittoria COLOTTA, Daniela CATARZI, Katia VARANI, Pier Andrea BOREA, Fabrizio VINCENZI
-
Patent number: 8222275Abstract: 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.Type: GrantFiled: July 2, 2007Date of Patent: July 17, 2012Assignee: Pharmeste S.R.L.Inventors: Pier Giovanni Baraldi, Pier Andrea Borea, Pierangelo Geppetti, Maria Giovanna Pavani, Francesca Fruttarolo, Marcello Trevisani
-
Patent number: 7964642Abstract: The invention relates to compounds of formula (I), wherein R, R1, R2, X and n are as defined in the description, and their use for the preparation of pharmaceutical compositions for the treatment of inflammatory states.Type: GrantFiled: June 16, 2005Date of Patent: June 21, 2011Assignee: Pharmeste S.R.L.Inventors: Pier Giovanni Baraldi, Pier Andrea Borea, Pierangelo Geppetti
-
Patent number: 7919624Abstract: 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.Type: GrantFiled: July 2, 2007Date of Patent: April 5, 2011Assignee: Pharmeste S.R.L.Inventors: Pier Giovanni Baraldi, Pier Andrea Borea, Pierangelo Geppetti, Maria Giovanna Pavani, Francesca Fruttarolo, Marcello Trevisani
-
Patent number: 7767685Abstract: The present invention provides compounds of the formula which are adenosine A2B receptor antagonists and, thus, may be employed for the treatment of conditions and diseases mediated by the adenosine A2B receptor 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 A2B receptors, e.g.Type: GrantFiled: June 25, 2007Date of Patent: August 3, 2010Assignee: King Pharmaceuticals Research and Development, Inc.Inventors: Pier Giovanni Baraldi, Pier Andrea Borea, Allan Moorman, Mojgan Aghazadeh Tabrizi
-
Patent number: 7750049Abstract: The invention relates to compounds of formula (I) in which R is selected from halogen, alkyl, alkoxy, aryl and heteroaryl; R1 is 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. R2 is 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.Type: GrantFiled: December 6, 2007Date of Patent: July 6, 2010Assignee: Pharmeste S.R.L.Inventors: Pier Giovanni Baraldi, Pier Andrea Borea, Pierangelo Geppetti, Francesca Fruttarolo, Maria Giovanna Pavani, Marcello Trevisani
-
Publication number: 20100105740Abstract: The invention relates to compounds of formula (I) in which R is selected from halogen, alkyl, alkoxy, aryl and heteroaryl; R1 is 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-car-boxy-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.Type: ApplicationFiled: December 6, 2007Publication date: April 29, 2010Inventors: Pier Giovanni Baraldi, Pier Andrea Borea, Pierangelo Geppetti, Francesca Fruttarolo, Maria Giovanna Pavani, Marcello Trevisani
-
Patent number: 7691825Abstract: The present invention provides compounds of the formula wherein R1, R2, R3 and n have meaning as described in the specification, methods for their preparation, and pharmaceutical compositions containing them. The compounds of formula (I) are adenosine A2B receptor agonists and, thus, may be employed for the treatment of diseases in mammals that are mediated by the A2B receptor 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.Type: GrantFiled: June 4, 2007Date of Patent: April 6, 2010Assignee: King Pharmaceuticals Research and Development, Inc.Inventors: Pier Giovanni Baraldi, Pier Andrea Borea, Allan R. Moorman, Delia Preti
-
Publication number: 20100035923Abstract: 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.Type: ApplicationFiled: July 2, 2007Publication date: February 11, 2010Inventors: Pier Giovanni Baraldi, Pier Andrea Borea, Pierangelo Geppetti, Maria Giovanna Pavani, Francesca Fruttarolo, Marcello Trevisani
-
Publication number: 20090233878Abstract: The present invention provides compounds of the formula wherein Ar, R and R1 have a meaning as defined herein in the specification. Compounds of formula (I) are agonists of the A3 adenosine receptor and, thus, may be employed for the treatment of conditions mediated by the A3 adenosine receptor. Accordingly, the compounds of formula (I) may be employed for treatment of behavioral depression, cerebral ischemia, hypotension, chemically induced seizures, inflammatory diseases, asthma, and cancer diseases expressing the adenosine A3 receptor.Type: ApplicationFiled: August 29, 2008Publication date: September 17, 2009Inventors: Pier Giovanni Baraldi, Allan R. Moorman, Pier Andrea Borea
-
Patent number: 7579378Abstract: The invention relates to sulfonamido derivatives of formula (I) wherein R1-R7 are 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.Type: GrantFiled: October 18, 2005Date of Patent: August 25, 2009Assignee: Pharmeste S.R.L.Inventors: Pier Giovanni Baraldi, Pier Andrea Borea, Pierangelo Geppetti
-
Publication number: 20090203719Abstract: The present invention discloses the use of high affinity adenosine A3 receptor antagonists for enhancing chemotherapeutic treatment of cancers expressing adenosine A3 receptors and cancers expressing P-glycoprotein or MRP. In preferred embodiments, adenosine A3 receptor antagonists are administered before or during administration of a taxane family, vinca alkaloid, camptothecin or antibiotic chemotherapeutic agent.Type: ApplicationFiled: December 18, 2008Publication date: August 13, 2009Inventors: Pier Andrea Borea, Pier Giovanni Baraldi, Shih-Fong Chen, Edward Leung
-
Publication number: 20090118374Abstract: The invention relates to sulfonamido derivatives of formula (I) wherein R1-R7 are 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.Type: ApplicationFiled: October 18, 2005Publication date: May 7, 2009Inventors: Pier Giovanni Baraldi, Pier Andrea Borea, Pierangelo Geppetti
-
Patent number: 7470698Abstract: The compounds of the following formula: wherein R, R2, R3 and A have the meanings given in the specification, are endowed with selective A3 adenosine receptor antagonist activity. These compounds can be used in a pharmaceutical composition to treat disorders caused by excessive activation of the A3 receptor, or can be used in a diagnostic application to determine the relative binding of other compounds to the A3 receptor. 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 A3 receptors.Type: GrantFiled: July 9, 2007Date of Patent: December 30, 2008Assignee: King Pharmaceuticals Research and Development, Inc.Inventors: Pier Giovanni Baraldi, Pier Andrea Borea
-
Patent number: 7435740Abstract: A class of novel antagonists for the adenosine A3 receptor are disclosed. These compounds are useful as therapeutic agents for a number of diseases and medical conditions that are mediated by the A3 receptor. The compounds of this invention are also useful as diagnostic agents for the A3 receptor.Type: GrantFiled: January 31, 2006Date of Patent: October 14, 2008Assignee: King Pharmaceuticals Research and Development, Inc.Inventors: Pier Giovanni Baraldi, Pier Andrea Borea, Delia Preti, Mojgan Aghazadeh Tabrizi
-
Publication number: 20080085936Abstract: The invention relates to compounds of formula (I), wherein R, R1, R2, X and n are as defined in the description, and their use for the preparation of pharmaceutical compositions for the treatment of inflammatory states.Type: ApplicationFiled: June 16, 2005Publication date: April 10, 2008Inventors: Pier Giovanni BARALDI, Pier Andrea BOREA, Pierangelo GEPPETTI
-
Publication number: 20080045549Abstract: The present invention provides compounds of the formula which are adenosine A2B receptor antagonists and, thus, may be employed for the treatment of conditions and diseases mediated by the adenosine A2B receptor 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, non-insulin dependent 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 A2B receptors, e.g.Type: ApplicationFiled: June 25, 2007Publication date: February 21, 2008Inventors: Pier Giovanni Baraldi, Pier Andrea Borea, Allan Moorman, Mojgan Aghazadeh Tabrizi
-
Patent number: 7271171Abstract: The compounds of the following formula: wherein R, R2, R3 and A have the meanings given in the specification, are endowed with selective A3 adenosine receptor antagonist activity. These compounds can be used in a pharmaceutical composition to treat disorders caused by excessive activation of the A3 receptor, or can be used in a diagnostic application to determine the relative binding of other compounds to the A3 receptor. 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 A3 receptors.Type: GrantFiled: June 27, 2005Date of Patent: September 18, 2007Assignee: King Pharmaceuticals Research and Development, Inc.Inventors: Pier Giovanni Baraldi, Pier Andrea Borea
-
Patent number: 7064204Abstract: New compounds having a tricyclic pyrazolotriazolopyrimidine ring structure are provided and methods of using those compounds for a variety of therapeutic indications.Type: GrantFiled: May 30, 2003Date of Patent: June 20, 2006Assignee: King Pharmacueticals Reserch and Development, Inc.Inventors: Pier Giovanni Baraldi, Pier Andrea Borea
-
Patent number: 6921825Abstract: The compounds of the following formula: wherein R, R2, R3 and A have the meanings given in the specification, are endowed with selective A3 adenosine receptor antagonist activity. These compounds can be used in a pharmaceutical composition to treat disorders caused by excessive activation of the A3 receptor, or can be used in a diagnostic application to determine the relative binding of other compounds to the A3 receptor. 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 A3 receptors.Type: GrantFiled: April 26, 2002Date of Patent: July 26, 2005Assignee: King Pharmaceuticuals Research & Development, Inc.Inventors: Pier Giovanni Baraldi, Pier Andrea Borea