Patents by Inventor Antonio Longo
Antonio Longo 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: 5965563Abstract: Novel bicyclic condensed pyrimidine compounds having general formula (I) ##STR1## wherein X is --CH.sub.2 --, --NH--(CH.sub.2).sub.n --, --O--(CH.sub.2).sub.n -- or --S--(CH.sub.2).sub.n -- in which n is zero or 1; A is a 4,5-fused imidazole ring N-substituted by R.sub.3 which is hydrogen, C.sub.1 -C.sub.4 alkyl or benzyl, or A is a 2,3-fused pyridine ring C-substituted by R.sub.4 which is hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, halogen or NR.sub.5 R.sub.6 in which each of R.sub.5 and R.sub.6 independently is H or C.sub.1 -C.sub.4 alkyl; B is a bicyclic ring chosen from tetralin, indane and 2-oxindole; each of R.sub.1 and R.sub.2 independently is hydrogen, C.sub.1 -C.sub.4 alkyl, halogen, hydroxy, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkoxycarbonyl, nitro, cyano or CF.sub.3 ; and the pharmaceutically acceptable salts thereof.Type: GrantFiled: July 14, 1997Date of Patent: October 12, 1999Assignee: Pharmacia & Upjohn S.p.A.Inventors: Franco Buzzetti, Maria Gabriella Brasca, Antonio Longo, Dario Ballinari
-
Patent number: 5840745Abstract: Novel hydrosoluble 3-arylidene-2-oxindole derivatives, having tyrosine kinase inhibitor activity, encompassed by general formula (I), wherein m is zero, 1 or 2; A is a bicyclic ring chosen from tetralin, naphthalene, quinoline and indole; R.sup.1 is hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.2 -C.sub.6 alkanoyl; one of R.sup.2 and R.sup.3 independently is hydrogen and the other is a substituent selected from: a C.sub.1 -C.sub.6 alkyl group substituted by 1, 2 or 3 hydroxy groups; --SO.sub.3 R.sup.4 in which R.sup.4 is hydrogen or C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by 1, 2 or 3 hydroxy groups; --SO.sub.2 NHR.sup.5 in which R.sup.5 is as R.sup.4 defined above or a --(CH.sub.2).sub.n --N(C.sub.1 -C.sub.6 alkyl).sub.2 group in which n is 2 or 3; --COOR.sup.6 in which R.sup.6 is C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by phenyl or by 1, 2 or 3 hydroxy groups or phenyl; --CONHR.sup.7 in which R.sup.7 is hydrogen, phenyl or C.sub.1 -C.sub.Type: GrantFiled: September 25, 1996Date of Patent: November 24, 1998Assignee: Pharmacia S. p. A.Inventors: Franco Buzzetti, Maria Gabriella Brasca, Antonio Longo, Dario Ballinari
-
Patent number: 5719135Abstract: The present invention relates to compound of formula (I) ##STR1## wherein A is benzene, naphthalene, 5,6,7,8,-tetrahydronaphthalene, quinoline, isoquinoline, indole or 7-azaindole;R.sub.1 is --H, --CN, --SO.sub.3 R.sub.4 --, --SO.sub.2 NHR.sub.5, ##STR2## --COOR.sub.6, --CONHCH.sub.2 (CHOH).sub.n CH.sub.2 OH, ##STR3## --NR.sub.7 R.sub.8, --N(CH.sub.2 CH.sub.2 OH).sub.2, --NHCH.sub.2 (CHOH).sub.n CH.sub.2 OH, --NHCONH.sub.2, --NH--C(NH.sub.2).dbd.NH, --NHCO(CHOH).sub.n CH.sub.2 OH, ##STR4## --NHSO.sub.2 R.sub.9, --OR.sub.10, --OCH.sub.2 (CHOH).sub.n CH.sub.2 OH, --OOC(CHOH).sub.n CH.sub.2 OH, --OPO(OH).sub.2, --CH.sub.2 NH.sub.2, --C(NH.sub.2).dbd.NH, --CH.sub.2 NHC(NH.sub.2).dbd.NH, ##STR5## --CH.sub.2 OH, --CH.sub.2 OOC(CHOH).sub.n CH.sub.2 OH, --CH.sub.2 OPO(OH).sub.2 or --PO(OH).sub.2 ;R.sub.2 is C.sub.1 -C.sub.6 alkyl, halogen, or hydroxy;R.sub.3 is --H or C.sub.1 -C.sub.6 alkyl;R.sub.4 is --H, C.sub.1 -C.sub.6 alkyl or --CH.sub.2 (CHOH).sub.n CH.sub.2 OH;R.sub.5 is --H, C.sub.1 -C.sub.6 alkyl, --CH.sub.Type: GrantFiled: July 9, 1996Date of Patent: February 17, 1998Assignee: Pharmacia S.p.A.Inventors: Franco Buzzetti, Gabriella Maria Brasca, Antonio Longo, Dario Ballinari
-
Patent number: 5663346Abstract: The present invention relates to compounds useful as tyrosine kinase inhibitors, having the following general formula (I) ##STR1## wherein one of the groups X.sup.1, X.sup.2, X.sup.3, X.sup.4 is N and the others are CH; R is a group of formula (a), (b), (c) or (d) ##STR2## each of R.sup.1 and R.sup.3 independently is hydrogen, amino, carboxy, cyano, --SO.sub.3 R.sup.4, --SO.sub.2 NHR.sup.5, ##STR3## --COOR.sup.6, --CONH(CH.sub.2).sub.o Ph, --CONHCH.sub.2 (CHOH).sub.n CH.sub.2 OH, ##STR4## --N (CH.sub.2 CH.sub.2 OH).sub.2, --NHCH.sub.2 (CHOH).sub.n CH.sub.2 OH, --NHCONH.sub.2, --NHC(NH.sub.2).dbd.NH, --NHCO(CHOH).sub.n CH.sub.2 OH, ##STR5## --NHSO.sub.2 R.sup.7, --OCH.sub.2 (CHOH).sub.n CH.sub.2 OH, --OOC(CHOH).sub.n CH.sub.2 OH, --OPO(OH).sub.2, --OCH.sub.2 SO.sub.2 NH.sub.2, --CH.sub.2 NH.sub.2, --C(NH.sub.2).dbd.NH, --CH.sub.2 NHC(NH.sub.2).dbd.NH, ##STR6## --CH.sub.2 OH, --CH.sub.2 OOC(CHOH).sub.n C.sub.2 OH, --CH.sub.2 OPO(OH).sub.2, --PO(OH).sub.2 ;R.sup.2 is H, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.Type: GrantFiled: February 9, 1996Date of Patent: September 2, 1997Assignee: Pharmacia S.p.A.Inventors: Franco Buzzetti, Maria Gabriella Brasca, Antonio Longo, Dario Ballinari
-
Patent number: 5656654Abstract: Arylidene and heteroarylidene oxindole derivatives of formula (I) ##STR1## wherein, subject to provisos, Y is a bicyclic ring system chosen from naphthalene, tetralin, quinoline and isoquinoline;R is hydrogen or an oxo (.dbd.O) group when Y is tetralin; orR is hydrogen when Y is naphthalene, quinoline or isoquinoline;each of R.sup.1 and R.sup.2 independently is hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.2 -C.sub.6 alkanoyl;m is zero, 1 or 2;n is zero, 1, 2 or 3;each of R.sup.3 and R.sup.4 independently is hydrogen, halogen, cyano, C.sub.1 -C.sub.6 alkyl, carboxy, nitro or --NR.sup.6 R.sup.7 in which each of R.sup.6 and R.sup.7 independently is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sup.5 is hydrogen or C.sub.1 -C.sub.6 alkyl; and their pharmaceutically acceptable salts, which are useful as tyrosine kinase inhibitors.Type: GrantFiled: June 22, 1994Date of Patent: August 12, 1997Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Franco Buzzetti, Antonio Longo, Maria Gabriella Brasca, Fabrizio Orzi, Angelo Crugnola, Dario Ballinari, Mariangela Mariani
-
Patent number: 5652250Abstract: The present invention relates to new compounds of formula ##STR1## wherein A is a bicyclic ring chosen from naphthalene, tetrahydronaphthalene, quinoline, isoquinoline and indole.B is a R.sup.2 substituted benzene ring or an unsubstituted pyridine or thiophene ring;R is hydrogen, C.sub.1 -C.sub.6 alkyl, halogen, nitro, cyano, carboxy or a group NR.sup.3 R.sup.4 wherein each of R.sup.3 and R.sup.4 is independently hydrogen or C.sub.1 -C.sub.6 alkyl;R.sup.1 is hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.1 -C.sub.6 alkanoyl;R.sup.2 is hydrogen, C.sub.1 -C.sub.6 alkyl, halogen, nitro, cyano, carboxy, hydroxy, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkanoyloxy or a group NR.sup.3 R.sup.4 wherein R.sup.3 and R.sup.4 are as defined above;n is zero or an integer of 1 to 2;x is zero or an integer of 1 to 5;and the pharmaceutically acceptable salts thereof.The compounds of the invention are useful as tyrosine kinase inhibitors.Type: GrantFiled: November 21, 1995Date of Patent: July 29, 1997Assignee: Pharmacia S.p.A.Inventors: Franco Buzzetti, Angelo Crugnola, Antonio Longo, Maria Gabriella Brasca, Dario Ballinari
-
Patent number: 5627207Abstract: The present invention provides compounds of the formula ##STR1## wherein Y is a naphthyl, tetrahydronaphthyl, pyridyl, quinolyl, isoquinolyl or indolyl ring system, R is a moiety which is an acrylic acid, a CN-substituted acrylic acid, acrylamide, acrylonitrile or thioacrylamide, or a group of formulae (e) to (j): ##STR2## wherein R.sub.3 is OH or NH.sub.2, R.sub.1 is H, alkyl or alkanoyl, R.sub.2 is H, halogen, CN or alkyl; and n is 0, 1, 2 or 3; and the pharmaceutically acceptable salts thereof are useful as tyrosine kinase inhibitors.Type: GrantFiled: May 31, 1995Date of Patent: May 6, 1997Assignee: Farmitalia Carlo Erba S r lInventors: Franco Buzzetti, Antonio Longo, Maristella Colombo
-
Patent number: 5576330Abstract: The new use of a compound of formula (I) ##STR1## wherein Y is a bicyclic ring selected from naphthalene, tetralin, quinoline, isoquinoline and indole;n is zero or an integer of 1 to 3;R.sub.1 is hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.2 -C.sub.6 alkanoyl;R.sub.2 is hydrogen, halogen, C.sub.1 -C.sub.6 alkyl, cyano, carboxy, nitro, or NHR, wherein R is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.3 is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.4 is hydrogen, hydroxy, C.sub.1 -C.sub.6 alkoxy, C.sub.2 -C.sub.6 alkanoyloxy, carboxy, nitro or NHR, wherein R is as defined above;R.sub.5 is hydrogen, C.sub.1 -C.sub.6 alkyl or halogen; or a pharmaceutically acceptable salt thereof;and wherein when Y is naphthalene then n is zero or an integer of 1 to 3, whereas when Y is tetralin, quinoline, isoquinoline or indole then n is zero, 1 or 2; and wherein when the bicyclic ring Y is naphthalene, quinoline, isoquinoline or indole, then each of the substituents OR.sub.1, R.sub.Type: GrantFiled: December 12, 1994Date of Patent: November 19, 1996Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Franco Buzzetti, Antonio Longo, Maria G. Brasca, Fabrizio Orzi, Angelo Crugnola, Dario Ballinari, Mariangela Mariani
-
Patent number: 5502044Abstract: The present invention relates to a compound of formula (I) ##STR1## wherein (x) and (y) are single or double bonds; A is a ##STR2## R and R.sup.3 are hydrogen or acyl; R.sup.1 is hydrogen or fluorine;and wherein:when (y) is a single bond, R.sup.2 is hydrogen, fluorine methyl, trifluoromethyl;when (y) is a double bond, R.sup.2 is methylene provided that when one of (x) or (y) is a double bond the other is a single bond and at least one of R.sub.1 and R.sub.2 is fluorine or trifluoromethyl or a pharmaceutically acceptable salt thereof. The compounds of formula (I) are useful as aromatase inhibitors.Type: GrantFiled: February 14, 1994Date of Patent: March 26, 1996Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Franco Buzzetti, Antonio Longo, Enrico Di Salle
-
Patent number: 5488057Abstract: The present invention provides novel aryl- and heteroarylethenylene derivatives which are useful as tyrosine kinase activity inhibitors.Type: GrantFiled: August 23, 1994Date of Patent: January 30, 1996Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Franco Buzzetti, Antonio Longo, Maristella Colombo
-
Patent number: 5457097Abstract: This invention refers to compounds of formula (I) ##STR1## wherein x, y, z represent single or double bonds;R is hydrogen or C.sub.1 -C.sub.4 alkyl;R.sub.1 is hydrogen or an acyl group;R.sub.2 is hydrogen; C.sub.1 -C.sub.4 alkyl unsubstituted or substituted by phenyl; phenyl unsubstituted or substituted by C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy; andA is a >C.dbd.O, >CH OH or >CH OR.sub.3 group, in which R.sub.3 is an acyl group provided that one of z and y is a double bond and the other is a single bond.The compounds are useful as aromatase inhibitors.Type: GrantFiled: July 19, 1993Date of Patent: October 10, 1995Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Franco Buzzetti, Antonio Longo, Enrico Di Salle
-
Patent number: 5409949Abstract: The invention provides new methylen-indole derivatives of formula (I) ##STR1## wherein R is a group ##STR2## in which R.sub.4 is hydrogen, hydroxy, C.sub.1 -C.sub.6 alkoxy, C.sub.2 -C.sub.6 alkanoyloxy, carboxy, nitro or NHR.sub.7, wherein R.sub.7 is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.5 is hydrogen, C.sub.1 -C.sub.6 alkyl or halogen; andR.sub.6 is hydrogen or C.sub.1 -C.sub.6 alkyl;n is zero, 1 or 2;R.sub.1 is hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.2 -C.sub.6 alkanoyl;R.sub.2 is hydrogen, C.sub.1 -C.sub.6 alkyl, halogen, cyano, carboxyl, nitro or --NHR.sub.7 in which R.sub.7 is as defined above;R.sub.3 is hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.2 -C.sub.6 alkanoyl; and the pharmaceutically acceptable salts thereof; and wherein, when, at the same time, R.sub.2 is hydrogen, C.sub.1 -C.sub.6 alkyl, halogen or cyano and R.sub.3 is hydrogen, R.sub.1 and n being as defined above, then at least one of R.sub.4, R.sub.5 and R.sub.6 is other than hydrogen, which are useful as tyrosine kinase inhibitors.Type: GrantFiled: March 12, 1993Date of Patent: April 25, 1995Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Franco Buzzetti, Antonio Longo, Maristella Colombo
-
Patent number: 5374652Abstract: Aryl- and heteroarylethenylene derivatives of formula ##STR1## wherein Y is a mono- or bicyclic ring system chosen from (A), (B), (C), (D), (E), (F) and (G) ##STR2## R is a group of formula R.sub.1 is hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.2 -C.sub.6 alkanoyl; R.sub.2 is hydrogen, halogen, cyano or C.sub.1 -C.sub.6 alkyl;n is zero or an integer of 1 to 3: n is zero or an integer of 1 to 3 when Y is a ring system (A); it is zero, 1 or 2 when Y is a ring system (B), (E), (F) or (G); or it is zero or 1 when Y is a ring system (C) or (D); and the pharmaceutically acceptable salts thereof; and wherein each of the substituents R, OR.sub.1 and R.sub.2 may be independently on either of the aryl or heteroaryl moieties of the bicyclic ring system (A), (E), (F) and (G), whereas only the benzene moiety may be substituted in the bicyclic ring system (B), are useful as tyrosine kinase activity inhibitors.Type: GrantFiled: September 27, 1993Date of Patent: December 20, 1994Assignee: Farmitalia Carlo Erba S r lInventors: Franco Buzzetti, Antonio Longo, Maristella Colombo
-
Patent number: 5241090Abstract: 4-amino-unsaturated androstanedione derivatives provided with aromatase inhibitory activity are obtained by hydrolyzation of a corresponding compound of formula II ##STR1##Type: GrantFiled: May 20, 1992Date of Patent: August 31, 1993Assignee: Farmitalia Carlo Erba S.R.L.Inventors: Fabrizio Orzi, Antonio Longo, Matteo D'Anello, Natale Barbugian
-
Patent number: 5080906Abstract: The blood level of orally administered N-acetylcysteine is substantially increased in a mammal when the N-acetylcysteine is administered in combination with tris(hydroxymethyl)aminomethane or a pharmaceutically acceptable salt thereof, in a molar ratio of about 1:0.8 to about l:l.2.Type: GrantFiled: July 27, 1990Date of Patent: January 14, 1992Assignee: Zambon Group, S.p.A.Inventors: Angelo Carenzi, Dario Chiarino, Antonio Longo
-
Patent number: 4990635Abstract: The invention relates to a new process for the preparation of known aromatase inhibitors of the following formula (I) ##STR1## wherein each of R.sub.1 and R.sub.3, independently, is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.2 is hydrogen, halogen or C.sub.1 -C.sub.6 alkyl; andR.sub.4 is hydrogen or fluorine;the process comprising submitting to Mannich reaction a compound of formula (II) ##STR2## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are as defined above and R is a lower alkyl group, and then dehydrogenating the respective 6-methylene-3-oxo-.DELTA..sup.4 -steroid derivative thus obtained, by methods known per se.Type: GrantFiled: January 6, 1989Date of Patent: February 5, 1991Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Antonio Longo, Paolo Lombardi
-
Patent number: 4970327Abstract: The invention relates to a new process for the preparation of know aromatase inhibitors of the following formula (I) ##STR1## wherein each of R.sub.1 R.sub.3, independently, is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.2 is hydrogen, halogen or C.sub.1 -C.sub.6 alkyl; andR.sub.4 is hydrogen or fluorine;the process comprising submitting to Mannich reaction a compound of formula (II) ##STR2## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are defined above and R is a lower alkyl group, and then dehydrogenating the respective 6-methylene-3-oxo-.DELTA..sup.4 -steroid derivative thus obtained, by methods known per se.Type: GrantFiled: January 6, 1989Date of Patent: November 13, 1990Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Antonio Longo, Paolo Lombardi
-
Patent number: 4876045Abstract: The invention relates to a new process for the preparation of known aromatase inhibitors of the following formula ##STR1## wherein each of R.sub.1 and R.sub.3, independently, is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.2 is hydrogen, halogen or C.sub.1 -C.sub.6 alkyl andR.sub.4 is hydrogen or fluorine; the process comprising subjecting to Mannich reaction a compound of formula ##STR2## wherein R.sub.1,R.sub.2,R.sub.3 and R.sub.4 are as defined above, and then oxidizing the respective 6-methylene derivative thus obtained by methods known per se.Type: GrantFiled: September 12, 1988Date of Patent: October 24, 1989Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Antonio Longo, Paolo Lombardi
-
Patent number: 4869900Abstract: A pharmaceutical composition, comprising: Coenzyme Q.sub.10 (ubidecarenone) 2-17% by weight; Lecithin 50-70% by weight; Surfactant agent 20-48% by weight. The surfactant agent has a melting point comprised between 35.degree. and 55.degree. C. and a HLB value from 12 to 15. Said composition provides a high absorption of Coenzime Q.sub.10. Solid pharmaceutical preparations containing the above composition are described too.Type: GrantFiled: November 6, 1986Date of Patent: September 26, 1989Assignee: Zambon S.p.A.Inventors: Franco Pozzi, Antonio Longo, Angelo Carenzi
-
Patent number: 4865766Abstract: A process for the preparation of 4-aminoandrostenediones of formula (I) ##STR1## and pharmaceutically acceptable salts thereof, wherein one of R.sub.1 and R.sub.2 is hydrogen and the other is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl or C.sub.2 -C.sub.6 alkynyl, and the symbol indicates that each of (x) and (y), independently, is a single bond or a double bond, comprising reacting a compound of formula (II) ##STR2## wherein E is a halogen atom and R.sub.1, R.sub.2, (x) and (y) each are as defined as above with ammonia.Type: GrantFiled: May 10, 1988Date of Patent: September 12, 1989Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Antonio Longo, Fabrizio Orzi, Paolo Lombardi, Maristella Colombo