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).

  • Patent number: 8609659
    Abstract: 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: Grant
    Filed: December 13, 2010
    Date of Patent: December 17, 2013
    Assignee: Neuroscienze Pharmaness S.C.A.R.L.
    Inventors: Paolo Lazzari, Giovanni Loriga, Stefania Ruiu, Gabriele Murineddu, Luca Pani, Gerard Aime Pinna
  • Patent number: 8399457
    Abstract: 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: Grant
    Filed: July 30, 2009
    Date of Patent: March 19, 2013
    Assignee: Neuroscienze Pharmaness S.C. A.R.L.
    Inventors: Paolo Lazzari, Giovanni Loriga, Stefania Ruiu, Ilaria Manca, Luca Pani, Gerard Aime Pinna
  • Publication number: 20130017149
    Abstract: 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: Application
    Filed: September 14, 2012
    Publication date: January 17, 2013
    Applicant: NEUROSCIENZE PHARMANESS S.C. A.R.L.
    Inventors: Paolo LAZZARI, Giovanni Loriga, Ilaria Manca, Gerard Aime Pinna, Luca Pani
  • Patent number: 8227620
    Abstract: 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: Grant
    Filed: December 22, 2009
    Date of Patent: July 24, 2012
    Assignee: Neuroscienze Pharmaness S.C. A.R.L.
    Inventors: Paolo Lazzari, Stefania Ruiu, Gerard Aime Pinna, Gabriele Murineddu
  • Publication number: 20120088751
    Abstract: 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: Application
    Filed: December 16, 2011
    Publication date: April 12, 2012
    Applicant: NEUROSCIENCZE PHARMANESS S.C. A R.L.
    Inventors: Paolo LAZZARI, Stefania RUIU, Gerard Aime PINNA, Gabrielle MURINEDDU
  • Patent number: 8106218
    Abstract: 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: Grant
    Filed: December 8, 2008
    Date of Patent: January 31, 2012
    Assignee: Neuroscienze Pharmaness S.C. A R.L.
    Inventors: Paolo Lazzari, Stefania Ruiu, Gerard Aime Pinna, Gabriele Murineddu
  • Publication number: 20110152238
    Abstract: 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: Application
    Filed: December 13, 2010
    Publication date: June 23, 2011
    Applicant: NEUROSCIENZE PHARMANESS S.C. A.R.L.
    Inventors: Paolo LAZZARI, Giovanni Loriga, Stefania Ruiu, Gabrieie Murineddu, Luca Pani, Gerard Aime Pinna
  • Publication number: 20100215741
    Abstract: 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: Application
    Filed: February 25, 2010
    Publication date: August 26, 2010
    Applicant: NEUROSCIENZE PHARMANESS S.C. A.R.L.
    Inventors: Paolo LAZZARI, Giovanni Loriga, Ilaria Manca, Gerard Aime Pinna, Luca Pani
  • Publication number: 20100215759
    Abstract: 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: Application
    Filed: February 25, 2010
    Publication date: August 26, 2010
    Applicant: NEUROSCIENZE PHARMANESS S.C.A.R.L.
    Inventors: Paolo LAZZARI, Giovanni Loriga, Ilaria Manca, Gerard Aime Pinna
  • Publication number: 20100216785
    Abstract: 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: Application
    Filed: February 25, 2010
    Publication date: August 26, 2010
    Applicant: NEUROSCIENZE PHARMANESS S.C. A.R.L.
    Inventors: Paolo LAZZARI, Giovanni LORIGA, Ilaria MANCA, Gerard Aime PINNA, Luca PANI
  • Publication number: 20100105896
    Abstract: 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: Application
    Filed: December 22, 2009
    Publication date: April 29, 2010
    Applicant: Neuroscienze Pharmaness S.C.a.R.I.
    Inventors: Paolo Lazzari, Stefania Rulu, Gerard Aime Pinna, Gabriele Murineddu
  • Patent number: 7659407
    Abstract: 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: Grant
    Filed: May 23, 2005
    Date of Patent: February 9, 2010
    Assignee: Neuroscienze Pharmaness S.C.a.R.I.
    Inventors: Paolo Lazzari, Stefania Ruiu, Gerard Aime Pinna, Gabriele Murineddu
  • Publication number: 20100028257
    Abstract: 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: Application
    Filed: July 30, 2009
    Publication date: February 4, 2010
    Applicant: NEUROSCIENZE PHARMANESS S.C. A.R.L.
    Inventors: Paolo LAZZARI, Giovanni LORIGA, Stefania RUIU, Ilaria MANCA, Luca PANI, Gerard Aime PINNA
  • Publication number: 20100029622
    Abstract: 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: Application
    Filed: July 30, 2009
    Publication date: February 4, 2010
    Applicant: NEUROSCIENZE PHARMANESS S.C.A.R.L.
    Inventors: Paolo LAZZARI, Giovanni Loriga, Stefania Ruiu, Ilaria Manca, Luca Pani, Gerard Aime Pinna
  • Publication number: 20090081123
    Abstract: 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: Application
    Filed: December 8, 2008
    Publication date: March 26, 2009
    Applicant: CeNeRx BioPharma
    Inventors: Paolo LAZZARI, Stefania RUIU, Gerard Aime PINNA, Gabriele MURINEDDU
  • Patent number: 7485730
    Abstract: 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: Grant
    Filed: May 23, 2005
    Date of Patent: February 3, 2009
    Assignee: Neuroscienze Pharmaness S.C. A R.L.
    Inventors: Paolo Lazzari, Stefania Ruiu, Gerard Aime Pinna, Gabriele Murineddu
  • Publication number: 20030195217
    Abstract: 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: Application
    Filed: May 20, 2003
    Publication date: October 16, 2003
    Inventors: Giorgio Cignarella, Gerard Aime Pinna