Patents by Inventor Fabrizio Micheli

Fabrizio Micheli 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: 7745458
    Abstract: The present invention relates to novel compounds of formula (I) or a salt thereof: wherein: p is 0, 1, 2, 3, 4 or 5; R1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl and SF5; n is 3 or 4; R2 is hydrogen or C1-4alkyl; n is 2 or 3; X is —CH2—, —O— or —S—; Z may be —CH— or N; A is a group P or P1, wherein P is and P1 is and Y is hydrogen, —OH, C1-4alkyl, haloC1-4alkyl, phenyl or a heteroaromatic group, wherein the phenyl and the heteroaromatic group are optionally substituted by one or two substituents selected from a group consisting of C1-4alkyl, haloC1-4alkyl, C1-4alkoxy and haloC1-4alkoxy; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as modulators of dopamine D3 receptors, e.g. to treat substance related disorders, as antipsychotic agents premature ejaculation or cognition impairment.
    Type: Grant
    Filed: August 18, 2006
    Date of Patent: June 29, 2010
    Assignee: Glaxo Group Limited
    Inventors: Luca Arista, Anna Checchia, Gabriella Gentile, Dieter Hamprecht, Fabrizio Micheli
  • Publication number: 20100160336
    Abstract: The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt thereof: wherein G is selected from a group consisting of: phenyl, pyridyl, benzothiazolyl, indazolyl; p is an integer ranging from 0 to 5; R1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl; or corresponds to a group R5; R2 is hydrogen or C1-4alkyl; R3 is C1-4alkyl; R4 is hydrogen, or a phenyl group, a heterocyclyl group, a 5- or 6-membered heteroaromatic group, or a 8- to 11-membered bicyclic group, any of which groups is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl; R5 is a moiety selected from the group consisting of: isoxazolyl, —CH2—N-pyrrolyl, 1,1-dioxido-2-isothiazolidinyl, thienyl, thiazolyl, pyridyl, 2-pyrrolidinonyl, and such a group is optionally substituted by one or two substituent
    Type: Application
    Filed: December 16, 2009
    Publication date: June 24, 2010
    Inventors: Luca Arista, Giorgio Bonanomi, Anna Maria Capelli, Federica Damiani, Romano Di Fabio, Gabriella Gentile, Dieter Hamprecht, Fabrizio Micheli, Luca Tarsi, Giovanna Tedesco, Silvia Terreni
  • Publication number: 20100152195
    Abstract: The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt thereof: wherein G is selected from a group consisting of: phenyl, pyridyl, benzothiazolyl, indazolyl; p is an integer ranging from 0 to 5; R1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl; or corresponds to a group R5; R2 is hydrogen or C1-4alkyl; R3 is C1-4alkyl; R4 is hydrogen, or a phenyl group, a heterocyclyl group, a 5- or 6-membered heteroaromatic group, or a 8- to 11-membered bicyclic group, any of which groups is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl; R5 is a moiety selected from the group consisting of: isoxazolyl, —CH2—N-pyrrolyl, 1,1-dioxido-2-isothiazolidinyl, thienyl, thiazolyl, pyridyl, 2-pyrrolidinonyl, and such a group is optionally substituted by one or two substituent
    Type: Application
    Filed: December 16, 2009
    Publication date: June 17, 2010
    Inventors: Luca Arista, Giorgio Bonanomi, Anna Maria Capelli, Federica Damiani, Romano Di Fabio, Gabriella Gentile, Dieter Hamprecht, Fabrizio Micheli, Luca Tarsi, Giovanna Tedesco, Silvia Terreni
  • Patent number: 7727988
    Abstract: The present invention relates to novel compounds of formula (I)? or a salt thereof: wherein G is selected from a group consisting of: phenyl, a 5- or 6-membered monocyclic heteroaryl group, or a 8- to 11-membered heteroaryl bicyclic group; A is a group P1 or a group P2 wherein P1 is and the other groups are define in herein.
    Type: Grant
    Filed: March 30, 2007
    Date of Patent: June 1, 2010
    Assignee: Glaxo Group Limited
    Inventors: Barbara Bertani, Giorgio Bonanomi, Anna Maria Capelli, Anna Checchia, Romano Di Fabio, Gabriella Gentile, Fabrizio Micheli, Alessandra Pasquarello, Giovanna Tedesco, Silvia Terreni
  • Publication number: 20100063078
    Abstract: The present invention relates to novel compounds of formula (I) or salts thereof: wherein A is a substituent selected in the group consisting of P, P1, P2 and P3 wherein P is P1 is P2 is P3 is p is an integer ranging from 0 to 4; R4 is selected in the group consisting of halogen, hydroxy, cyano, C1-4 alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl, SF5 and a 5- or 6-membered monocyclic heteroaryl group; and when p is an integer ranging from 2 to 4, each R4 may be the same or different; R2 is hydrogen or C1-4alkyl; q is 3, 4 or 5; n is 0, 1 or 2; X is —CR1R3— or —O—; R1 is selected in the group consisting of hydrogen, C1-4 alkyl and fluorine; R3 is selected in the group consisting of hydrogen, C1-4alkyl and fluorine; R5 is selected in the group consisting of: hydrogen, halogen, hydroxy, cyano, C1-4alkyl, C3-7 cycloalkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl and NR?R?; or R5 is a phenyl group, a 5-14 membered heterocyclic group; and any of such phenyl or hetero
    Type: Application
    Filed: April 24, 2007
    Publication date: March 11, 2010
    Inventors: Barbara Bertani, Romano Di Fabio, Fabrizio Micheli, Alessandra Pasquarello, Luca Tarsi, Silvia Terreni
  • Publication number: 20100063097
    Abstract: The present invention relates to certain azabicyclic compounds of formula (I)?: wherein the several groups are defined herein and are modulators of dopamine D3 receptors, e.g. to treat drug dependency, as antipsychotic agents, to treat obsessive compulsive spectrum disorders, or premature ejaculation.
    Type: Application
    Filed: March 30, 2007
    Publication date: March 11, 2010
    Inventors: Barbara Bertani, Fabrizio Micheli, Alessandra Pasquarello, Silvia Terreni
  • Publication number: 20100035914
    Abstract: The present invention relates to novel compounds of formula (I)?, and pharmaceutically acceptable salts, prodrugs or solvates thereof: wherein R1 is hydrogen or C1-4 alkyl; R2 is a group A, K or W wherein A is K is an ? or ? naphthyl group, optionally substituted by 1 or 2 groups R18, each of them being the same or different; and W is and wherein G is a 5,6-membered monocyclic heteroaryl group, or a 8- to 11-membered heteroaryl bicyclic group; wherein G may be substituted by (R15)p, which can be the same or different; p is an integer from 0 to 5; R3 is selected from the group consisting of: hydrogen, fluorine, and C1-4 alkyl; or corresponds to a group X or X1; R4 is selected from the group consisting of: hydrogen, fluorine, and C1-4 alkyl; or corresponds to a group X or X1; R5 is hydrogen or C1-4 alkyl; R7 is hydrogen or C1-4 alkyl; or is a group X, X1, X2 or X3; wherein X is X1 is X2 is and X3 is R6 is hydrogen or C1-4 alkyl; or is a group X or X1; R9 is C1-4a
    Type: Application
    Filed: September 7, 2007
    Publication date: February 11, 2010
    Inventors: Barbara Bertani, Romano Di Fabio, Fabrizio Micheli, Giovanna Tedesco, Silvia Terreni
  • Publication number: 20100029740
    Abstract: Novel compounds of formula (I)? and pharmaceutically acceptable salts, solvates and prodrugs thereof: wherein A is: K is a mono or bicyclic aryl group; R1 is selected from halogen, C1-4alkyl and C1-4alkoxy (R1 may assume different meanings on the basis of p value); p is an integer from 0 to 5; R2 is a group P: R3 is hydrogen, C1-4alkyl, C3-6cycloalkyl, C3-6cycloalkylC1-3alkyl, haloC1-2alkyl or an optionally substituted phenyl group; X is oxygen, —NR8— or sulphur; n is 0 or 1; R7 is hydrogen or methyl; R8 is hydrogen or C1-4alkyl; R4 is hydrogen or methyl; R5 is hydrogen or C1-4alkyl; and R6 is hydrogen or C1-4alkyl; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as serotonin (5-HT), dopamine (DA) and norepinephrine (NE), re-uptake inhibitors.
    Type: Application
    Filed: December 12, 2007
    Publication date: February 4, 2010
    Inventors: Giorgio Bonanomi, Fabrizio Micheli, Silvia Terreni
  • Publication number: 20100016287
    Abstract: Compounds of formula (I) wherein A is a 5 or 6 membered heteroaromatic ring or a 5 or 6 membered heterocyclic ring, and which are useful for treating mental disorders such as schizophrenia are set out herein.
    Type: Application
    Filed: May 31, 2005
    Publication date: January 21, 2010
    Applicant: GLAXO GROUP LIMITED
    Inventors: Giorgio Bonanomi, Federica Damiani, Gabriella Gentile, Dieter Wolfgang Hamprecht, Fabrizio Micheli, Luca Tarsi, Giovanna Tedesco, Silvia Terreni
  • Publication number: 20090326011
    Abstract: Disclosed herein are compounds of formula (I) where G and Q are heteroaromatic groups. These compounds are useful for treating psychosis or a psychotic condition, substance abuse, premature ejaculation or cognition impairment.
    Type: Application
    Filed: June 13, 2006
    Publication date: December 31, 2009
    Inventors: Luca Arista, Francesca Cardullo, Anna Checchia, Dieter Hamprecht, Fabrizio Micheli, Giovanna Tedesco, Silvia Terreni
  • Publication number: 20090281135
    Abstract: The present invention relates to novel compounds of formula (I) or pharmaceutically acceptable salts, solvates or prodrugs thereof: wherein G is selected from the group consisting of: phenyl, a 5- or 6-membered monocyclic heteroaryl group, and a 8- to 11-membered heteroaryl bicyclic group; wherein G may be substituted by (R2)p, which can be the same or different; R1 is hydrogen or C1-4 alkyl; R2 is halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl or SF5; or corresponds to R8; R5 is hydrogen or C1-4 alkyl; R6 is hydrogen or C1-4 alkyl; R7 is selected from the group consisting of: hydrogen, fluorine, and C1-4 alkyl; or corresponds to X, X1, X2 or X3; wherein X corresponds to: X1 corresponds to: X2 corresponds to: X3 corresponds to: R3 is hydrogen or C1-4 alkyl; or corresponds to X or X1; R4 is hydrogen or C1-4 alkyl; or corresponds to X or X1; R8 is a 5-6 membered heterocycle group, which may be substituted by one or two substituents select
    Type: Application
    Filed: September 7, 2007
    Publication date: November 12, 2009
    Inventors: Romano Di Fabio, Fabrizio Micheli, Giovanna Tedesco, Silvia Terreni
  • Publication number: 20090221618
    Abstract: The present invention relates to novel compounds of formula (I) or a salt thereof: wherein: p is 0, 1, 2, 3, 4 or 5; R1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl and SF5; n is 3 or 4; R2 is hydrogen or C1-4alkyl; n is 2 or 3; X is —CH2—, —O— or —S—; Z may be —CH— or N; A is a group P or P1, wherein P is and P1 is ; and Y is hydrogen, —OH, C1-4alkyl, haloC1-4alkyl, phenyl or a heteroaromatic group, wherein the phenyl and the heteroaromatic group are optionally substituted by one or two substituents selected from a group consisting of C1-4alkyl, haloC1-4alkyl, C1-4alkoxy and haloC1-4alkoxy; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as modulators of dopamine D3 receptors, e.g. to treat substance related disorders, as antipsychotic agents premature ejaculation or cognition impairment.
    Type: Application
    Filed: August 18, 2006
    Publication date: September 3, 2009
    Inventors: Luca Arista, Anna Checchia, Gabriella Gentile, Dieter Hamprecht, Fabrizio Micheli
  • Publication number: 20090221593
    Abstract: The present invention relates to novel compounds of formula (I) or a salt thereof: wherein: G is a 5- or 6-membered heteroaromatic group, or is a 9- or 10-membered bicyclic heteroaromatic group containing one or two heteroatoms independently selected from nitrogen and oxygen, wherein G is not pyridyl, indazolyl or benzothiazolyl; p is an integer ranging from 0 to 4; R1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl or SF5; or corresponds to a group R5; R2 is hydrogen or C1-4alkyl; n is 2 or 3; X is S or —CH2—; R3 is C1-4alkyl; R4 is hydrogen, or a phenyl group, a heterocyclyl group, a 5- or 6-membered heteroaromatic group, or a 8- to 11-membered bicyclic group, any of which groups is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy and C1-4alkanoyl; R5 is isoxazolyl, —CH2—N-pyrrolyl, 1,1-dioxido-2-isothiazolidin
    Type: Application
    Filed: August 18, 2006
    Publication date: September 3, 2009
    Inventors: Giorgio Bonanomi, Romano Di Fabio, Elettra Fazzolari, Dieter Hamprecht, Fabrizio Micheli, Luca Tarsi, Silvia Terreni
  • Publication number: 20090036461
    Abstract: The present invention provides a new use of a compound of formula (I) or a pharmaceutically acceptable salt or solvate salt thereof: wherein: G is selected from a group consisting of: phenyl, pyridyl, benzothiazolyl, indazolyl; p is an integer ranging from 0 to 5; R1 is independently selected from a group consisting of: halogen, hydroxyl, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl; or corresponds to a group R5; R2 is hydrogen or C1-4alkyl; R3I s C1-4alkyl; R4 is hydrogen, or a phenyl group, a heterocyclyl group, a 5- or 6-membered heteroaromatic group, or a 8- to 11-membered bicyclic group, any of which groups is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl; R5 is a moiety selected from the group consisting of: isoxazolyl, —CH2—N-pyrrolyl, 1,1-dioxido-2-isothiazolidinyl, thienyl, thiazolyl, pyridyl, 2-pyrrolidinonyl, and such a group is optionally substituted by
    Type: Application
    Filed: August 21, 2006
    Publication date: February 5, 2009
    Inventors: Dieter Hamprecht, Christian Heidbreder, Sergio Melotto, Fabrizio Micheli, Tadataka Yamada
  • Publication number: 20090030062
    Abstract: The present invention relates to novel compounds of formula (IA) or a salt thereof: wherein: A is attached to the phenyl group at the meta position or the para position relative to the cyclopropyl group, and is selected from the group consisting of: —SO2NR5—, —SO2CR2R3—, —CR2R3SO2— and —NR5SO2—; R1 is hydrogen, C1-6alkyl, haloC1-6alkyl or C2-6alkylene; R2 and R3 are independently hydrogen or C1-6alkyl; R4 is hydrogen, halogen, C1-6alkyl, haloC1-6alkyl, C1-6alkoxy or haloC1-6alkoxy; R5 is hydrogen, C1-6alkyl, or a phenyl optionally substituted by R4; and R6 is hydrogen, C1-6alkyl, haloC1-6alkyl, C1-6alkoxy or haloC1-6alkoxy; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as modulators of dopamine D3 receptors, e.g. to treat substance related disorders, as antipsychotic agents premature ejaculation or cognition impairment.
    Type: Application
    Filed: August 18, 2006
    Publication date: January 29, 2009
    Inventors: Gabriella Gentile, Dieter Hamprecht, Fabrizio Micheli, Adolfo Prandi, Silvia Terreni
  • Publication number: 20080312213
    Abstract: Compounds of formula (I) or a salt thereof are disclosed: wherein R1 is pyrazolyl substituted by two or three substituents independently selected from halogen, C1-4alkyl and haloC1-4alkyl; R2 is hydrogen or methyl; and R3 is quinolinyl, oxazolyl or phenyl, each of which is optionally substituted by one or two halogen, C1-4alkyl or haloC1-4alkyl. Processes for preparation and uses of the compounds in medicine, for example for the treatment of schizophrenia or drug dependency, are also disclosed.
    Type: Application
    Filed: June 17, 2005
    Publication date: December 18, 2008
    Applicant: GLAXO GROUP LIMITED
    Inventors: Dieter Hamprecht, Fabrizio Micheli, Luca Tarsi, Giovanna Tedesco
  • Patent number: 7462622
    Abstract: The present invention provides compounds of formula (I) including stereoisomers, prodrugs and pharmaceutically acceptable salts or solvates thereof wherein R is aryl or heteroaryl and each of the above groups R may be substituted by 1 to 4 groups selected from: halogen, C1-C6 alkyl, C1-C6 alkoxy, halo C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkoxy, —COR4, nitro, —NR3R4 cyano, or a group R5; R1 is hydrogen, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkyl, halo C1-C6 alkoxy, halogen, NR3R4 or cyano; R2 corresponds to a group CHR6R7; R3 is hydrogen, C1-C6 alkyl; R4 independently from R3, has the same meanings; R5 is C3-C7 cycloalkyl, which may contain one or more double bonds; aryl; or a 5-6 membered heterocycle; ?wherein each of the above groups R5 may be substituted by one or more groups selected from: halogen, C1-C6 alkyl, C1-C6 alkoxy, halo C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkoxy, C1-C6 dialkylamino, nitro or cyano; R6 is hydrogen, C2-C6 alkenyl or C1-
    Type: Grant
    Filed: June 11, 2002
    Date of Patent: December 9, 2008
    Assignee: Glaxo Group Limited
    Inventors: Romano Di Fabio, Chiara Marchionni, Fabrizio Micheli, Alessandra Pasquarello, Bendetta Perini, Yves St-Denis
  • Publication number: 20080269195
    Abstract: Compounds of formula (I) or a salt thereof are disclosed: wherein, A, m R1, R2, R3, q, W1, W2, R4 and R5 are as defined in the description. Processes for preparation and uses of the compounds in medicine, for example for the treatment of schizophrenia or drug dependency, are also disclosed.
    Type: Application
    Filed: June 29, 2005
    Publication date: October 30, 2008
    Inventors: Giorgio Bonanomi, Francesca Cardullo, Federica Damiani, Gabriella Gentile, Dieter Hamprecht, Fabrizio Micheli, Luca Tarsi
  • Publication number: 20080242715
    Abstract: The present invention relates to novel compounds of formula (IC) or a salt thereof: wherein: p is an integer ranging from 0 to 4; R1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl or SF5; or corresponds to a group R5; m1, m2, m3, and m4 are 0; m5, m6 and m7 are each independently 0, 1 or 2 wherein the sum of m5, m6 and m7 is 1 or 2; R6 is C1-6alkyl; R7 is halogen, C1-6alkyl or haloC1-6alkyl; R2 is hydrogen or C1-4alkyl; n is 2 or 3; X is S or —CH2—; R3 is C1-4alkyl; R4 is hydrogen, or a phenyl group, a heterocyclyl group, a 5- or 6-membered heteroaromatic group, or a 8- to 11-membered bicyclic group, any of which groups is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy and C1-4alkanoyl; R5 is isoxazolyl, —CH2—N-pyrrolyl, 1,1-dioxido-2-isothiazolidinyl, thienyl, thiazolyl, pyridyl or 2-pyrrolidinonyl,
    Type: Application
    Filed: August 18, 2006
    Publication date: October 2, 2008
    Inventors: Anna Marie Capelli, Elettra Fazzolari, Fabrizio Micheli, Giovanna Tedesco, Silvia Terreni
  • Publication number: 20080176917
    Abstract: The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt thereof: wherein R1 is hydrogen or C1-4alkyl; R2 is C1-4alkyl; R3 is hydrogen, or a phenyl group, a heterocyclyl group, a 5- or 6-membered heteroaromatic group, or a 8- to 11-membered bicyclic group, any of which groups is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl and SF5; p is 0, 1, 2, 3 or 4; and R4 is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy and C1-4alkanoyl; n is 0 or 1; wherein when R4 is chlorine and p is 1, such R4 is not present in the ortho position with respect to the linking bond to the rest of the molecule; and wherein, if n is 0, R3 comprises at least one SF5 group as a substituent; processes for their preparation, intermediates used in these processes, pharmaceutical compositions contai
    Type: Application
    Filed: April 12, 2006
    Publication date: July 24, 2008
    Inventors: Daniele Andreotti, Anna Checchia, Dieter Hamprecht, Fabrizio Micheli