Patents by Inventor Gerard Aime Pinna
Gerard Aime Pinna 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).
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Patent number: 8609659Abstract: Diazapolycyclic compounds having affinity for the opioidergic receptors, preferably for the delta opioidergic receptors, with central and/or peripheral activity, having formula: A1-D1-T1??(I) wherein: A1 is a group of formula (II): wherein: R1 is phenyl wherein one of the ring hydrogen atoms is substituted with a group selected from C(O)R?, C(O)OR?, C(O)NHR? or C(O)NR3R4, R?, R3 and R4, being as defined in the application; R2 is phenyl, optionally substituted D1 is a diazapolycyclic group T1 is a group selected from H, alkyl, alkenyl, alkynyl and from the following optionally substituted groups: cycloalkyl, heterocycloalkyl, aryl, heteroaryl, cycloalkylalkyl, heterocycloalkylalkyl, arylalkyl or heteroarylalkyl, and their hydrates and solvates and pharmaceutically acceptable salts.Type: GrantFiled: December 13, 2010Date of Patent: December 17, 2013Assignee: Neuroscienze Pharmaness S.C.A.R.L.Inventors: Paolo Lazzari, Giovanni Loriga, Stefania Ruiu, Gabriele Murineddu, Luca Pani, Gerard Aime Pinna
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Patent number: 8399457Abstract: Nonane and decane diazabicyclic derivatives having homopiperazine as main ring, having affinity for the opioidergic ? and/or ? and/or k receptors and/or for all their receptorial subclasses, with central and/or peripheral activity, having formula (I), the isomeric forms and their mixtures included, wherein one or more atoms are in the corresponding isotopic forms: wherein: n is an integer equal to 1 or 2; one of the substituents R and R1 of the nitrogen atoms of the diazabicyclic ring is a —C(O)—RB group, wherein RB is a C1-C10 alkyl group, linear or branched when possible, the other remained substituent of R and R1 has the meanings reported in the description.Type: GrantFiled: July 30, 2009Date of Patent: March 19, 2013Assignee: Neuroscienze Pharmaness S.C. A.R.L.Inventors: Paolo Lazzari, Giovanni Loriga, Stefania Ruiu, Ilaria Manca, Luca Pani, Gerard Aime Pinna
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Publication number: 20130017149Abstract: Condensed tricyclic compounds having a condensed structure containing one phenyl and one pyrazole ring linked with each other by a central ring comprising from five to eight atoms, having affinity for the CB1 and/or CB2 receptors, with central nervous system and/or peripheral activity, of formula (I): wherein the various substituents are as defined in the description. The compounds show affinity for the CB1 and/or CB2 cannabinoidergic receptors.Type: ApplicationFiled: September 14, 2012Publication date: January 17, 2013Applicant: NEUROSCIENZE PHARMANESS S.C. A.R.L.Inventors: Paolo LAZZARI, Giovanni Loriga, Ilaria Manca, Gerard Aime Pinna, Luca Pani
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Patent number: 8227620Abstract: Pyrazole derivatives of the following formula (I), having affinity for the cannabinoidergic CB1 and/or CB2 receptors: wherein: R is a group selected from C1-C10 alkyl; aryl, arylalkyl or arylalkenyl, not substituted or having from one to four substituents, equal to or different from each other; A is a group selected from the following: an ether group of formula —(CH2)—O—(CH2)v—R? wherein v is equal to 1 or 2; R? is as defined in the present application; a ketone group of formula —C(O)—Z?, wherein Z? is as defined in the present application; a substituent having an hydroxyl function of formula —CH(OH)—Z?, being as defined in the present application; an amide substituent of formula —C(O)—NH-T?, T? being as defined in the present application; B is a group as defined in the present application; D is an heteroaryl optionally substituted.Type: GrantFiled: December 22, 2009Date of Patent: July 24, 2012Assignee: Neuroscienze Pharmaness S.C. A.R.L.Inventors: Paolo Lazzari, Stefania Ruiu, Gerard Aime Pinna, Gabriele Murineddu
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Publication number: 20120088751Abstract: Tricyclic pyrazole derivatives of the following formula (I) having affinity for the cannabinoidergic CB1 and/or CB2 receptors: wherein: A represents a group selected from one of the following: (CH2)t—, —(CH2)—S(O)z—, or —S(O)z—(CH2)—, B is a heteroaryl, optionally substituted; R is a group selected from the following: alkyl, aryl, arylalkyl or arylalkenyl, not substituted or having from one to four substituents, equal to or different from each other; R? is a group selected from the following: an ether group of formula —(CH2)—O—(CH2)v—R?, a ketonic group of formula —C(O)—Z?, wherein Z? is as defined below; a substituent having an hydroxyl function of formula —CH(OH)—Z?; an amide substituent of formula —C(O)—NH-T?.Type: ApplicationFiled: December 16, 2011Publication date: April 12, 2012Applicant: NEUROSCIENCZE PHARMANESS S.C. A R.L.Inventors: Paolo LAZZARI, Stefania RUIU, Gerard Aime PINNA, Gabrielle MURINEDDU
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Patent number: 8106218Abstract: Tricyclic pyrazole derivatives of the following formula (I) having affinity for the cannabinoidergic CB1 and/or CB2 receptors: wherein: A represents a group selected from one of the following: (CH2)t—, —(CH2)—S(O)z—, or —S(O)z—(CH2)—, B is a heteroaryl, optionally substituted; R is a group selected from the following: alkyl, aryl, arylalkyl or arylalkenyl, not substituted or having from one to four substituents, equal to or different from each other; R? is a group selected from the following: an ether group of formula —(CH2)—O—(CH2)v—R?, a ketonic group of formula —C(O)—Z?, wherein Z? is as defined below; a substituent having an hydroxyl function of formula —CH(OH)—Z?; an amide substituent of formula —C(O)—NH-T?.Type: GrantFiled: December 8, 2008Date of Patent: January 31, 2012Assignee: Neuroscienze Pharmaness S.C. A R.L.Inventors: Paolo Lazzari, Stefania Ruiu, Gerard Aime Pinna, Gabriele Murineddu
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Publication number: 20110152238Abstract: Diazapolycyclic compounds having affinity for the opioidergic receptors, preferably for the delta opioidergic receptors, with central and/or peripheral activity, having formula: A1-D1-T1??(I) wherein: A1 is a group of formula (II): wherein: R1 is phenyl wherein one of the ring hydrogen atoms is substituted with a group selected from C(O)R?, C(O)OR?, C(O)NHR? or C(O)NR3R4, R?, R3 and R4, being as defined in the application; R2 is phenyl, optionally substituted D1 is a diazapolycyclic group T1 is a group selected from H, alkyl, alkenyl, alkynyl and from the following optionally substituted groups: cycloalkyl, heterocycloalkyl, aryl, heteroaryl, cycloalkylalkyl, heterocycloalkylalkyl, arylalkyl or heteroarylalkyl, and their hydrates and solvates and pharmaceutically acceptable salts.Type: ApplicationFiled: December 13, 2010Publication date: June 23, 2011Applicant: NEUROSCIENZE PHARMANESS S.C. A.R.L.Inventors: Paolo LAZZARI, Giovanni Loriga, Stefania Ruiu, Gabrieie Murineddu, Luca Pani, Gerard Aime Pinna
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Publication number: 20100215741Abstract: Condensed tricyclic compounds having a condensed structure containing one phenyl and one pyrazole ring linked with each other by a central ring comprising from five to eight atoms, having affinity for the CB1 and/or CB2 receptors, with central nervous system and/or peripheral activity, of formula (I): wherein the various substituents are as defined in the description. The compounds show affinity for the CB1 and/or CB2 cannabinoidergic receptors.Type: ApplicationFiled: February 25, 2010Publication date: August 26, 2010Applicant: NEUROSCIENZE PHARMANESS S.C. A.R.L.Inventors: Paolo LAZZARI, Giovanni Loriga, Ilaria Manca, Gerard Aime Pinna, Luca Pani
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Publication number: 20100215759Abstract: Condensed tricyclic pyrazole compounds having affinity for the CB1 and/or CB2 cannabinoidergic receptors, with activity both on the peripheral and central nervous system, of formula (I): wherein: A represents a group selected from —(CH2)t—, —(CH2)r—O—(CH2)s— and —(CH2)r—S(O)p—(CH2)s— B is an heteroaryl, R is a group selected from heteroaryl, heteroarylalkyl, aryl, arylalkyl, arylalkenyl or bivalent aliphatic chain, R? is a group selected from the following: R?1: a substituent bearing a keto group of formula —C(O)— (Z?)v—Z? R?2: a substituent having an hydroxylic function of formula —CH(OH)—(Z?)v-Z?, R?3: an amide substituent of formula —C(O)—NH—(Z?)v-T?.Type: ApplicationFiled: February 25, 2010Publication date: August 26, 2010Applicant: NEUROSCIENZE PHARMANESS S.C.A.R.L.Inventors: Paolo LAZZARI, Giovanni Loriga, Ilaria Manca, Gerard Aime Pinna
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Publication number: 20100216785Abstract: Microemulsions of pharmaceutical compositions comprising, the following components (% by weight), the sum of the components being 100%: S) from 0.01 to 95% of one or more compounds selected from surfactants, polymers, forming organized structures as: aggregates, micelles, liquid crystals, vesicles, in the liquid in which they are solubilized, O) from 0.01 to 95% of one or more oils selected from esters of C4-C32 acids or C4-C32 acids, PA) from 0.001 to 90% of compounds having affinity for the CB1 and/or CB2 cannabinoidergic receptors of formula A?: AD) from 0 to 60% by weight of one or more compounds selected from modifiers of the water and/or oil polarity, modifiers of the film curvature of component S), co-surfactants, water or a saline aqueous solution the difference to 100%, wherein the ratio by weight S)/PA) is lower than that of microemulsions wherein component O) is absent.Type: ApplicationFiled: February 25, 2010Publication date: August 26, 2010Applicant: NEUROSCIENZE PHARMANESS S.C. A.R.L.Inventors: Paolo LAZZARI, Giovanni LORIGA, Ilaria MANCA, Gerard Aime PINNA, Luca PANI
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Publication number: 20100105896Abstract: Pyrazole derivatives of the following formula (I), having affinity for the cannabinoidergic CB1 and/or CB2 receptors: wherein: R is a group selected from C1-C10 alkyl; aryl, arylalkyl or arylalkenyl, not substituted or having from one to four substituents, equal to or different from each other; A is a group selected from the following: an ether group of formula —(CH2)—O—(CH2)v—R? wherein v is equal to 1 or 2; R? is as defined in the present application; a ketone group of formula —C(O)—Z?, wherein Z? is as defined in the present application; a substituent having an hydroxyl function of formula —CH(OH)—Z?, being as defined in the present application; an amide substituent of formula —C(O)—NH-T?, T? being as defined in the present application; B is a group as defined in the present application; D is an heteroaryl optionally substituted.Type: ApplicationFiled: December 22, 2009Publication date: April 29, 2010Applicant: Neuroscienze Pharmaness S.C.a.R.I.Inventors: Paolo Lazzari, Stefania Rulu, Gerard Aime Pinna, Gabriele Murineddu
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Patent number: 7659407Abstract: Pyrazole derivatives of the following formula (I), having affinity for the cannabinoidergic CB1 and/or CB2 receptors: wherein: R is a group selected from: C1-C10 alkyl; aryl, arylalkyl or arylalkenyl, not substituted or having from one to four substituents, equal to or different from each other; A is a group selected from the following: an ether group of formula —(CH2)—O—(CH2)v—R? wherein v is equal to 1 or 2; R? is as defined in the present application; a ketone group of formula —C(O)—Z?, wherein Z? is as defined in the present application; a substituent having an hydroxyl function of formula —CH(OH)—Z?, Z? being as defined in the present application; an amide substituent of formula —C(O)—NH—T?, T? being as defined in the present application; B is a group as defined in the present application; D is an heteroaryl optionally substituted.Type: GrantFiled: May 23, 2005Date of Patent: February 9, 2010Assignee: Neuroscienze Pharmaness S.C.a.R.I.Inventors: Paolo Lazzari, Stefania Ruiu, Gerard Aime Pinna, Gabriele Murineddu
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Publication number: 20100028257Abstract: Nonane and decane diazabicyclic derivatives having homopiperazine as main ring, having affinity for the opioidergic ? and/or ? and/or k receptors and/or for all their receptorial subclasses, with central and/or peripheral activity, having formula (I), the isomeric forms and their mixtures included, wherein one or more atoms are in the corresponding isotopic forms: wherein: n is an integer equal to 1 or 2; one of the substituents R and R1 of the nitrogen atoms of the diazabicyclic ring is a —C(O)—RB group; wherein RB is a C1-C10 alkyl group, linear or branched when possible, the other remained substituent of R and R1 has the meanings reported in the description.Type: ApplicationFiled: July 30, 2009Publication date: February 4, 2010Applicant: NEUROSCIENZE PHARMANESS S.C. A.R.L.Inventors: Paolo LAZZARI, Giovanni LORIGA, Stefania RUIU, Ilaria MANCA, Luca PANI, Gerard Aime PINNA
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Publication number: 20100029622Abstract: Pharmaceutical compositions in the form of microemulsions comprising the following components, in amounts expressed as % by weight, the sum of the components being 100%: S) from 0.01 to 95% of one or more pharmaceutically acceptable compounds, selected from the following classes: surfactants; polymers forming organized structures as micelles, liquid crystals, vesicles in the liquid in which they are solubilized; 0) from 0.01 to 95% of one or more oils, PA) from 0.001 to 90% of diazabicyclic compounds having formula A?: wherein t, r, Y, W have the meanings reported in the description, AD) from 0 to 60% by weight of one or more compounds selected from the following classes: modifiers of water and/or oil polarity, modifiers of the curvature of the film of component S), co-surfactants, water from 0.01 to 99.9%.Type: ApplicationFiled: July 30, 2009Publication date: February 4, 2010Applicant: NEUROSCIENZE PHARMANESS S.C.A.R.L.Inventors: Paolo LAZZARI, Giovanni Loriga, Stefania Ruiu, Ilaria Manca, Luca Pani, Gerard Aime Pinna
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Publication number: 20090081123Abstract: Tricyclic pyrazole derivatives of the following formula (I) having affinity for the cannabinoidergic CB1 and/or CB2 receptors: wherein: A represents a group selected from one of the following: (CH2)t—, —(CH2)—S(O)z—, or —S(O)z—(CH2)—, B is a heteroaryl, optionally substituted; R is a group selected from the following: alkyl, aryl, arylalkyl or arylalkenyl, not substituted or having from one to four substituents, equal to or different from each other; R? is a group selected from the following: an ether group of formula —(CH2)—O—(CH2)v—R?, a ketonic group of formula —C(O)-Z?, wherein Z? is as defined below; a substituent having an hydroxyl function of formula —CH(OH)-Z?; an amide substituent of formula —C(O)—NH-T?.Type: ApplicationFiled: December 8, 2008Publication date: March 26, 2009Applicant: CeNeRx BioPharmaInventors: Paolo LAZZARI, Stefania RUIU, Gerard Aime PINNA, Gabriele MURINEDDU
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Patent number: 7485730Abstract: Tricyclic pyrazole derivatives of the following formula (I) having affinity for the cannabinoidergic CB1 and/or CB2 receptors: wherein: A represents a group selected from one of the following: (CH2)t—, —(CH2)—S(O)z—, or —S(O)z—(CH2)—, B is a heteroaryl, optionally substituted; R is a group selected from the following: alkyl, aryl, arylalkyl or arylalkenyl, not substituted or having from one to four substituents, equal to or different from each other; R? is a group selected from the following: an ether group of formula —(CH2)—O—(CH2)v—R?, a ketonic group of formula —C(O)-Z?, a substituent having an hydroxyl function of formula —CH(OH)-Z?; and an amide substituent of formula —C(O)—NH-T?.Type: GrantFiled: May 23, 2005Date of Patent: February 3, 2009Assignee: Neuroscienze Pharmaness S.C. A R.L.Inventors: Paolo Lazzari, Stefania Ruiu, Gerard Aime Pinna, Gabriele Murineddu
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Publication number: 20030195217Abstract: Compounds of formula (I) wherein R and R1, which are different from each other, are a straight or branched C2-C8 acyl group, have analgesic activity.Type: ApplicationFiled: May 20, 2003Publication date: October 16, 2003Inventors: Giorgio Cignarella, Gerard Aime Pinna