Patents by Inventor Mario Varasi

Mario Varasi 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: 6306903
    Abstract: The present invention relates to novel and known alpha-aminoamide compounds, to a process for their preparation, to pharmaceutical composition containing them and to their use as therapeutic agents. In particular, the compounds of the present invention are endowed with analgesic properties and are particularly useful for the treatment and alleviation of chronic and neuropathic pain.
    Type: Grant
    Filed: August 29, 2000
    Date of Patent: October 23, 2001
    Assignee: Newron Pharmaceuticals S.p.A.
    Inventors: Paolo Pevarello, Mario Varasi, Patricia Salvati, Claes Post
  • Patent number: 6303819
    Abstract: Compounds which are substituted 2-benzylamino-2-phenyl-acetamide compounds of formula (I) wherein: n is zero, 1, 2 or 3; X is —O—, —S—, —CH2— or —NH—; each of R, R1, R2 and R3, independently, is hydrogen, C1-C6 alkyl, halogen, hydroxy, C1-C6 alkoxy or trifluoromethyl; each of R4 and R5, independently, is hydrogen, C1-C6 alkyl or C3-C7 cycloalkyl; or pharmaceutically acceptable salts thereof, are useful in treating conditions such as chronic or neuropathic pain.
    Type: Grant
    Filed: September 11, 2000
    Date of Patent: October 16, 2001
    Assignee: Newron Pharmaceuticals S.p.A.
    Inventors: Paolo Pevarello, Mario Varasi, Patricia Salvati, Claes Post
  • Patent number: 6268362
    Abstract: A compound of formula (1), wherein R1 represents hydrogen, hydroxy, a group of formula OR7, wherein R7 is C1-C6 alkyl, C2-C6 alkenyl; R2 represents hydrogen, hydroxy, diethylamino, piperidino, tetrahydropyridino or morpholino, and either R3, taken alone, represtnts hydrogen or hydroxy, and R4 and R5, taken alone, independently represent hydrogen, hydroxy or, taken together with the carbon atom, represent a carbonyl group; or R3 and R4, taken together, represent a group of formula (A), wherein R8 and R9 represent a C1-C6 alkyl and R5 represents hydrogen; R6 represents hydrogen or a phenyl group, optionally substituted by methyl, methoxy or halogen and the pharnaceutically acceptable salt thereof, is useful in the treatment of amyloidosis. Processes for the preparation and pharmaceutical compositions are also described.
    Type: Grant
    Filed: September 7, 2000
    Date of Patent: July 31, 2001
    Assignee: Pharmacia & Upjohn SpA
    Inventors: Tiziano Bandiera, Daniele Fancelli, Mario Varasi, Michele Caruso, Jacqueline Lansen, Antonino Suarato
  • Publication number: 20010008947
    Abstract: Use in the prevention and/or in the treatment of neurodegenerative diseases of 2-amino-4-phenyl-4-oxo-butyric acid derivatives which act as kynureninase enzyme inhibitors and/or kynurenine-3-hydroxylase enzyme inhibitors.
    Type: Application
    Filed: October 14, 1997
    Publication date: July 19, 2001
    Inventors: MARIO VARASI, ANTONIO GIORDANI, CARMELA SPECIALE, MASSIMO CINI, ALBERTO BIANCHETTI
  • Patent number: 6218418
    Abstract: Compounds which are 3-amino-pyrazole derivatives represented by formula (I): where R is a C3-C6 cycloalkyl group, which may optionally be substituted by a straight or branched C1-C6 alkyl group, and R1 is a straight or branched C1-C6 alkyl group or a C2-C4 alkenyl, cycloalkyl, aryl, arylalkyl, arylcarbonyl, aryloxyalkyl and arylalkenyl, which may be optionally substituted; or a pharmaceutically acceptable salt thereof. The compounds are useful for the treatment of cancer, cell proliferative disorders, Alzheimer's disease, viral infections, auto-immune diseases or neurodegenerative diseases.
    Type: Grant
    Filed: September 22, 2000
    Date of Patent: April 17, 2001
    Assignees: Pharmacia & Upjohn S.p.A, Pharmacia & Upjohn Co.
    Inventors: Paolo Pevarello, Paolo Orsini, Gabriella Traquandi, Mario Varasi, Edward L. Fritzen, Martha A. Warpehoski, Betsy S. Pierce, Maria Gabriella Brasca
  • Patent number: 6207709
    Abstract: An N-substituted-2-amino-4-phenyl-4-oxo-butanoic acid compound of the formula (I): wherein X, Y, W and R are as defined herein.
    Type: Grant
    Filed: February 24, 1999
    Date of Patent: March 27, 2001
    Assignee: Pharmacia & Upjohn S.p.A.
    Inventors: Mario Varasi, Antonio Giordani, Massimo Cini, Carmela Speciale, Alberto Bianchetti
  • Patent number: 6133302
    Abstract: 5-(3-phenyl-3-oxo-propyl)-1H-tetrazole derivatives of formula (I) wherein each of R and R.sub.1, being the same or different, is hydrogen, halogen, hydroxy, trifluoromethyl, cyano, nitro, phenyl, benzyl, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio, SOR.sub.4 or SO.sub.2 R.sub.4 wherein R.sub.4 is C.sub.1 -C.sub.6 alkyl, --N(R.sub.5 R.sub.6) in which each of R.sub.5 and R.sub.6 is, independently, hydrogen, C.sub.1 -C.sub.6 alkyl, formyl or C.sub.2 -C.sub.6 acyl; R.sub.2 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, benzyl, phenyl; R.sub.3 is hydrogen, hydroxy, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, benzyl, phenyl or a group --N(R.sub.7 R.sub.8) in which each of R.sub.7 and R.sub.8 is, independently, hydrogen, C.sub.1 -C.sub.4 alkyl, benzyl, phenyl, or one of R.sub.7 and R.sub.8 is hydrogen and the other is COR.sub.9 wherein R.sub.9 is hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, phenyl or a group --N(R.sub.10 R.sub.11) in which R.sub.
    Type: Grant
    Filed: December 30, 1999
    Date of Patent: October 17, 2000
    Assignee: Pharmacia & Upjohn SpA
    Inventors: Paolo Pevarello, Antonio Giordani, Manuela Villa, Carmela Speciale, Mario Varasi
  • Patent number: 6114365
    Abstract: 2-amino-1,3-thiazole derivatives represented by formula (I) or (II): ##STR1## where R, R.sub.1, R.sub.2 and R.sub.3 are as defined herein, or pharmaceutically acceptable salts thereof, are useful in, for example, the treatment of cancer, cell proliferative disorders, Alzheimer's disease, viral infections, auto-immune diseases or neurodegenerative diseases.
    Type: Grant
    Filed: August 12, 1999
    Date of Patent: September 5, 2000
    Assignee: Pharmacia & Upjohn S.p.A.
    Inventors: Paolo Pevarello, Raffaella Amici, Manuela Villa, Barbara Salom, Anna Vulpetti, Mario Varasi
  • Patent number: 6087371
    Abstract: Ergoline derivative having formula (I) wherein R.sub.1 is hydrogen atom or C.sub.1-4 alkyl group; R.sub.2 is hydrogen, chlorine, or bromine atom, methyl or C.sub.1-4 alkylthio group; n is 0, 1 or 2; the substituent at position 8 is in .alpha. or .beta. configuration; Het represents an aromatic 5-membered heterocyclic ring, said ring having three heteroatoms which are the same or different and which are selected from the group consisting of sulfur, oxygen and nitrogen atom and X is hydrogen, chlorine or bromine or fluorine atom, or a pharmaceutically acceptable acid addition salt thereof are active at the Central Nervous System level. A process for their preparation is also described, as are pharmaceutical compositions containing them.
    Type: Grant
    Filed: August 17, 1998
    Date of Patent: July 11, 2000
    Assignee: Pharmacia & Upjohn S.p.A.
    Inventors: Sergio Mantegani, Tiziano Bandiera, Maurizio Meroni, Mario Varasi, Carla Caccia
  • Patent number: 6060483
    Abstract: The present invention provides the new use in the treatment of neurodegenerative diseases with ergoline derivatives of formula (I) ##STR1## wherein R.sub.1 represents a hydrogen atom or a linear or branched C.sub.1 -C.sub.5 alkyl or C.sub.2 -C.sub.5 alkenyl group optionally substituted with a C.sub.3 -C.sub.7 cycloalkyl, a hydroxy group or a R.sub.3 -substituted phenyl group wherein R.sub.3 is a hydroxy or a hydroxymethyl group; R.sub.2 represents a hydrogen atom or a linear or branched C.sub.1 -C.sub.5 alkyl or a C.sub.2 -C.sub.5 alkenyl group optionally substituted with a hydroxy group, or a R.sub.3 -substituted phenyl group wherein R.sub.3 is as above defined, or with a C.sub.1 -C.sub.5 alkoxy group; the symbols--at positions 2,3 and 8, 9 independently denote a single or double chemical bond and Z represents a group (CH.sub.2).sub.n OH, wherein n is 0 or an integer from 1 to 3, or a group C(R.sub.4).sub.2 OH wherein R.sub.4 is a C.sub.1 -C.sub.
    Type: Grant
    Filed: December 28, 1998
    Date of Patent: May 9, 2000
    Assignee: Pharmacia & Upjohn S.p.A.
    Inventors: Sergio Mantegani, Enzo Brambilla, Nicola Carfagna, Mario Varasi
  • Patent number: 6048896
    Abstract: 4-Phenyl-4-oxo-butenoic acid derivatives for use in the treatment of the human or animal body by therapy; particularly as kynurenine-3-hydroxylase inhibitors, in the prevention and/or treatment of a neurodegenerative disease wherein the inhibition of such an enzyme is needed. The present invention further comprises a selected class of the above mentioned 4-phenyl-4-oxo-butenoic acid derivatives, their pharmaceutically acceptable salts, a process for their preparation and pharmaceutical compositions containing them.
    Type: Grant
    Filed: May 4, 1998
    Date of Patent: April 11, 2000
    Assignee: Pharmacia & Upjohn S.p.A.
    Inventors: Antonio Giordani, Paolo Pevarello, Carmela Speciale, Mario Varasi
  • Patent number: 5973006
    Abstract: A fluoro-substituted benzoylpropionic acid compound of formula (I) either as a single optical isomer or as a mixture of optical isomers ##STR1## wherein R is hydroxy, amino, hydroxylamine, --OR', --NHR', N(R').sub.2 or --NHOR' in which R' is C.sub.1 -C.sub.6 alkyl or benzyl;or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: April 20, 1998
    Date of Patent: October 26, 1999
    Assignee: Pharmacia & Upjohn S.p.A.
    Inventors: Mario Varasi, Antonio Giordani, Carmela Speciale, Massimo Cini, Alberto Bianchetti
  • Patent number: 5968955
    Abstract: A Disubstituted piperidine compounds of formula (I), wherein R.sub.1 is hydrogen; bromo; chloro; a linear or branched C.sub.1 -C.sub.5 alkyl group; a linear or branched C.sub.1 -C.sub.5 alkoxy group; or an optionally substituted phenyl group; R.sub.2 is hydrogen, a linear or branched C.sub.1 -C.sub.5 alkyl group or an optionally substituted phenyl group; X is CH.sub.2, C.dbd.O, CHOH or C.dbd.NOH; R.sub.3 is hydrogen or a linear or branched C.sub.1 -C.sub.5 alkyl group; Y is a (CH.sub.2).sub.n group in which n is an integer from 0 to 4, CHOH, C.dbd.O or CH-A wherein A is an optionally substituted phenyl group; A is an optionally substituted phenyl group; W is hydrogen or hydroxy; stereoisomers thereof and their pharmaceutically acceptable salts. The compounds possess selective neuroprotective activity and are useful in the treatment of an acute or a degenerative CNS disease. A process is described for preparing the compounds and pharmaceutical compositions containing them.
    Type: Grant
    Filed: March 31, 1998
    Date of Patent: October 19, 1999
    Assignee: Pharmacia & Upjohn S.p.A.
    Inventors: Sergio Mantegani, Tiziano Bandiera, Manuela Villa, Mario Varasi, Carmela Speciale
  • Patent number: 5945454
    Abstract: Novel 2(4-substituted)-benzylamino-2-methyl-propanamides compounds, having CNS activity, of general formula (I) wherein: n is zero, 1, 2 or 3; X is --O--, --S--, --CH.sub.2 -- or --NH--; each of R and R.sub.1 independently is hydrogen, C.sub.1 -C.sub.6 alkyl, halogen, hydroxy, C.sub.1 -C.sub.4 alkoxy or trifluoromethyl; each of R.sub.2, R.sub.3 and R.sub.4 independently is hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.3 -C.sub.7 cycloalkyl; and the pharmacetically acceptable salts thereof, are disclosed.
    Type: Grant
    Filed: January 8, 1998
    Date of Patent: August 31, 1999
    Assignee: Pharmacia & Upjohn, S.P.A.
    Inventors: Paolo Pevarello, Raffaella Amici, Mario Varasi, Alberto Bonsignori, Patricia Salvati
  • Patent number: 5912242
    Abstract: The present invention relates to novel N-(4-substituted-benzyl)-2-aminolactams as therapeutic agents, pharmaceutical compositions and a process of preparation.
    Type: Grant
    Filed: January 8, 1998
    Date of Patent: June 15, 1999
    Assignee: Pharmacia & Upjohn S.p.A.
    Inventors: Paolo Pevarello, Raffaella Amici, Mario Varasi, Roberto Maj, Patricia Salvati
  • Patent number: 5874457
    Abstract: Novel 5-HT.sub.3 receptor antagonist compounds having following formula (I) ##STR1## wherein n is 1, 2 or 3;each of R, R.sub.1 and R.sub.2, which may be the same or different, is hydrogen, halogen, hydroxy, cyano, C.sub.1 -C.sub.6 alkyl, CF.sub.3, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio, formyl, C.sub.2 -C.sub.6 alkanoyl, carboxy, C.sub.1 -C.sub.6 alkoxy-carbonyl, nitro, --N (R.sub.4 R.sub.5) in which each of R.sub.4 and R.sub.5 independently is hydrogen, C.sub.1 -C.sub.6 alkyl, formyl or C.sub.2 -C.sub.6 alkanoyl; or a (R.sub.6 R.sub.7) N--SO.sub.2 group, in which each of R.sub.6 and R.sub.7 independently is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.3 is an imidazolyl group of formula ##STR2## wherein each of R.sub.8 and R.sub.10 which may be the same or different is hydrogen or C.sub.1 -C.sub.6 alkyl, R.sub.9 is hydrogen, C.sub.1 -C.sub.6 alkyl or a nitrogen protecting group; and the pharmaceutically acceptable salts thereof, are disclosed.
    Type: Grant
    Filed: January 24, 1996
    Date of Patent: February 23, 1999
    Assignee: Pharmacia & Upjohn S.p.A.
    Inventors: Mario Varasi, Franco Heidempergher, Carla Caccia, Patricia Salvati
  • Patent number: 5786508
    Abstract: The present invention relates to the use in the treatment of cognitive disorders associated with the aging processes of the brain and perinatal brain disorders of compounds which act as inhibitors of the enzyme kynurenine aminotransferase (KAT).The present invention also provides, as novel compounds, a selected class of KAT inhibitors which are the compounds of formula (IA) ##STR1## wherein R is halogen, C.sub.1 -C.sub.6 alkyl, C.sub.5 -C.sub.7 cycloalkyl, phenyl-C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.6 -C.sub.10 aryloxy, phenyl-C.sub.1 -C.sub.4 alkoxy or trifluoromethyl, andR.sub.1 is hydroxy, C.sub.1 -C.sub.6 alkoxy, amino, mono-C.sub.1 -C.sub.6 alkylamino, di-C.sub.1 -C.sub.6 alkylamino, hydroxylamino, C.sub.1 -C.sub.4 alkoxyamino or benzyloxyamino,with the provisos that:(i) when R.sub.1 is hydroxy and, at the same time, R is halogen, then this halogen is not fluorine; and(ii) when R.sub.1 is hydroxy and, at the same time, R is C.sub.1 -C.sub.6 alkyl, then this C.sub.1 -C.sub.
    Type: Grant
    Filed: April 6, 1995
    Date of Patent: July 28, 1998
    Assignees: Pharmacia & Upjohn S.p.A., University of Maryland at Baltimore
    Inventors: Robert Schwarcz, Mario Varasi, Arturo Della Torre, Carmela Speciale, Alberto Bianchetti
  • Patent number: 5783574
    Abstract: Novel 5-HT.sub.3 receptor antagonist compounds having following formula (I) ##STR1## wherein n is 1, 2 or 3;each of R, R.sub.1 and R.sub.2, which may be the same or different, is hydrogen, halogen, hydroxy, cyano, C.sub.1 -C.sub.6 alkyl, CF.sub.3, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio, formyl, C.sub.2 -C.sub.6 alkanoyl, carboxy, C.sub.1 -C.sub.6 alkoxy-carbonyl, nitro, --N (R.sub.4 R.sub.5) in which each of R.sub.4 and R.sub.5 independently is hydrogen, C.sub.1 -C.sub.6 alkyl, formyl or C.sub.2 -C.sub.6 alkanoyl; or a (R.sub.6 R.sub.7) N--SO.sub.2 group, in which each of R6 and R.sub.7 independently is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.3 is an imidazolyl group of formula ##STR2## wherein each of R.sub.8 and R.sub.10 which may be the same or different is hydrogen or C.sub.1 -C.sub.6 alkyl, R.sub.9 is hydrogen, C.sub.1 -C.sub.6 alkyl or a nitrogen protecting group; and the pharmaceutically acceptable salts thereof, are disclosed.
    Type: Grant
    Filed: January 24, 1996
    Date of Patent: July 21, 1998
    Assignee: Pharmacia & Upjohn S.p.A.
    Inventors: Mario Varasi, Franco Heidempergher, Carla Caccia, Patricia Salvati
  • Patent number: 5708030
    Abstract: The present invention relates to the use in the treatment of cognitive disorders associated with the aging processes of the brain and perinatal brain disorders of compounds which act as inhibitors of the enzyme kynurenine aminotransferase (KAT).
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: January 13, 1998
    Assignees: University of Maryland, Pharmacia & Upjohn S.p.A.
    Inventors: Robert Schwarcz, Mario Varasi, Arturo Della Torre, Carmela Speciale, Alberto Bianchetti
  • Patent number: 5637596
    Abstract: Novel 5-HT.sub.3 receptor antagonist compounds having the general formula (I) ##STR1## wherein each of R, R.sub.1 and R.sub.2, which may be the same or different, is hydrogen, halogen, hydroxy, cyano, C.sub.1 -C.sub.6 alkyl, CF.sub.3, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio, formyl, C.sub.2 -C.sub.6 alkanoyl, carboxy, C.sub.1 -C.sub.6 alkoxy-carbonyl, nitro, --N(R.sub.4 R.sub.5) in which each of R.sub.4 and R.sub.5 independently is hydrogen, C.sub.1 -C.sub.6 alkyl, formyl or C.sub.2 -C.sub.6 alkanoyl; or a (R.sub.6 R.sub.7)N--SO.sub.2 group, in which each of R.sub.6 and R.sub.7 independently is hydrogen or C.sub.1 -C.sub.6 alkyl; ##STR2## wherein n is an integer of 1 or 2 and R.sub.8 is hydrogen, C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by phenyl, C.sub.2 -C.sub.4 alkenyl, C.sub.2 -C.sub.4 alkynyl, formyl or C.sub.2 -C.sub.6 alkanoyl; and the pharmaceutically acceptable salts thereof, are provided.
    Type: Grant
    Filed: January 24, 1996
    Date of Patent: June 10, 1997
    Assignee: Pharmacia S.p.A.
    Inventors: Mario Varasi, Franco Heidempergher, Carla Caccia, Patricia Salvati