Patents by Inventor Ilaria Candiani
Ilaria Candiani 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: 5998426Abstract: The present invention relates to 9-amino-10-(1-naphthylsulfonyloxy)-20(S)-camptothecin, 9-amino-10-phenylsulfonyloxy-20(S)-camptothecin, 7-ethyl-9-amino-10-(p-toluensulfonyloxy)-20(S)-camptothecin, their pharmaceutically acceptable salts, a process for their preparation, pharmaceutically compositions comprising them and their use as antitumor agents.Type: GrantFiled: September 29, 1997Date of Patent: December 7, 1999Assignee: Pharmacia & Upjohn S.p.A.Inventors: Angelo Bedeschi, Walter Cabri, Ilaria Candiani, Franco Zarini, Sergio Penco
-
Patent number: 5990120Abstract: The present invention relates to novel hexacyclic camptohecin analogues, having a five-membered aza-heterocycle fused to ring (A) of camptothecin at positions 9 and 10. Such compounds possess high antitumor activity by inhibition of topoisomerase (I).Type: GrantFiled: September 10, 1997Date of Patent: November 23, 1999Assignee: Pharmacia & Upjohn S.p.A.Inventors: Angelo Bedeschi, Ilaria Candiani, Franco Zarini
-
Patent number: 5916897Abstract: The present invention relates to compounds of the following formulas: ##STR1## which are endowed with antitumor activity. The invention also relates to methods of treating tumors using these compounds.Type: GrantFiled: December 31, 1996Date of Patent: June 29, 1999Assignee: Pharmacia & Upjohn S.p.A.Inventors: Walter Cabri, Ilaria Candiani, Franco Zarini, Angelo Bedeschi, Sergio Penco
-
Patent number: 5856496Abstract: A process for preparing libraries of indole compounds by solid phase synthesis in the presence of organometallic catalysts. The resulting compounds have a very high purity degree, which allows biological testing on the crude products with a high confidence degree, without any cross contaminations.Type: GrantFiled: January 12, 1998Date of Patent: January 5, 1999Assignee: Pharmacia & Upjohn S.p.A.Inventors: Maria Chiara Fagnola, Angelo Bedeschi, Ilaria Candiani, Giuseppina Visentin, Nicola Mongelli
-
Patent number: 5856333Abstract: The present invention relates to substituted camptothecin derivatives of formula (I) wherein the symbol - - - - represents a single or double bond; R.sub.1, R.sub.2 and R.sub.3 are as defined under (a) or (b) below: (a) R.sub.1 and R.sub.2 are, each independently, hydrogen; C.sub.1 -C.sub.4 alkyl; C.sub.3 -C.sub.7 cycloalkyl; phenyl C.sub.1 -C.sub.6 alkyl; an optionally substituted phenyl ring; --NR.sub.5 R.sub.6 wherein one of R.sub.5 and R.sub.6 is hydrogen, C.sub.1 -C.sub.6 alkyl or benzyl and the other is hydrogen, C.sub.1 -C.sub.6 alkanoyl, an optionally substituted C.sub.1 -C.sub.6 alkoxycarbonyl, an optionally substituted benzoyl, phenyl C.sub.1 -C.sub.6 alkanoyl, an optionally substituted C.sub.1 -C.sub.6 alkoxycarbonyl, an optionally substituted phenoxycarbonyl or phenyl C.sub.1 -C.sub.6 alkoxycarbonyl, or R.sub.5 and R.sub.6, combined together with the nitrogen atom to which they are linked, form a 4-7 membered saturated, optionally substituted, heteromonocyclic ring residue; COOR.sub.8 wherein R.Type: GrantFiled: January 27, 1997Date of Patent: January 5, 1999Assignee: Pharmacia & Upjohn S.p.A.Inventors: Walter Cabri, Ilaria Candiani, Angelo Bedeschi, Franco Zarini, Sergio Penco
-
Patent number: 5840899Abstract: 9-Amino camptothecin of formula (I) ##STR1## is prepared by: 1) reducing a compound of formula (II): ##STR2## wherein Hal is 10- or 12-halogen, in a single step to the 9-amino-camptothecin of formula (I) or, alternatively, 2a) reductively removing the Hal group from a compound of formula (II) so obtaining the compound of formula (III): ##STR3## and 2b) reducing the compound of formula (III) so obtaining the 9-amino camptothecin of formula (I); the said steps 1 and 2a) and, optionally, step 2b) each being carried out in the presence of a catalytic amount of a compound of formula PdL.sub.2 wherein L is acetate or halogen and, additionally, in the presence of an ammonium formate as a hydrogen source. The 9-amino camptothecin of formula (I) is useful as inhibitor of the enzyme topoisomerase I. It is useful in the treatment of cancers, in particular leukaemia, colon and rectal tumours.Type: GrantFiled: September 30, 1996Date of Patent: November 24, 1998Assignee: Pharmacia S.p.A.Inventors: Angelo Bedeschi, Walter Cabri, Ilaria Candiani, Franco Zarini
-
Patent number: 5801167Abstract: The present invention relates to new camptothecin derivatives which display antitumor activity. The present invention also provides processes for their preparation as well as pharmaceutical compositions containing the same.Type: GrantFiled: August 20, 1996Date of Patent: September 1, 1998Assignee: Pharmacia S.p.A.Inventors: Angelo Bedeschi, Franco Zarini, Walter Cabri, Ilaria Candiani, Sergio Penco, Laura Capolongo
-
Patent number: 5614628Abstract: A process for preparing 9-amino camptothecin comprising the steps of: (1) reacting a compound of formula (III) ##STR1## wherein the hydroxy group on ring A is in the 10- or 12-position, with a nitrating agent, to form the corresponding 9-nitro compound; (2) converting the 9-nitro compound into a corresponding compound of formula (V) ##STR2## wherein XO is a group that can be removed reductively; and (3) reductively removing the XO group and reducing the nitro group of the compound of formula (V), to form the 9-amino camptothecin, a known antitumor compound. The present invention also includes compound having the above formula (V) and their 9-amino analogs, which have antitumor activity.Type: GrantFiled: September 28, 1994Date of Patent: March 25, 1997Assignee: Pharmacia & Upjohn S.p.A.Inventors: Walter Cabri, Ilaria Candiani, Franco Zarini, Angelo Bedeschi, Sergio Penco
-
Patent number: 5602141Abstract: The present invention relates to new camptothecin derivatives of the formula (I) ##STR1## wherein B is a group B' or B" ##STR2## wherein each of (x) and (y) is a single or double bond. The present invention also provides processes for their preparation as well as pharmaceutical compositions containing the same.Type: GrantFiled: February 15, 1995Date of Patent: February 11, 1997Assignee: Pharmacia & Upjohn S.P.A.Inventors: Angelo Bedeschi, Franco Zarini, Walter Cabri, Ilaria Candiani, Sergio Penco, Laura Capolongo
-
Patent number: 5459161Abstract: Substituted benzofuran derivatives of the formula (I): ##STR1## wherein one of R.sub.1 and R.sub.2 is hydrogen or halogen and the other is, independently, an amino group or a C.sub.2 -C.sub.4 alkanoyl amino group; R.sub.3 is hydrogen; a linear or branched C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy or C.sub.2 -C.sub.4 alkoxycarbonyl group; halogen; or phenyl unsubstituted or substituted by a C.sub.1 -C.sub.4 alkyl group; A is a group --(CH.sub.2).sub.n -Het wherein Het is an optionally substituted heteromonocyclic or heterobicyclic ring containing one or two nitrogen atoms, and n is zero or an integer of 1 to 3; and the symbol ..... represents a single or double bond; may be prepared by a process comprising reacting a compound of formula II: ##STR2## in which L is a leaving group and R.sub.4 is hydrogen or a carboxy protecting group, with a compound of formula III;R'.sub.3 --C.dbd.C--R'.sub.Type: GrantFiled: June 25, 1993Date of Patent: October 17, 1995Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Angelo Bedeschi, Walter Cabri, Ilaria Candiani, Silvia De Bernardinis, Marcello Marchi
-
Patent number: 5399679Abstract: There is provided a process for preparing a compound of formula (I) ##STR1## wherein R is H or a hydroxy protecting group, R.sub.2 is an organic residue and R.sub.3 is H or a nitrogen protecting group, which process comprises reacting together a compound of formula (II) ##STR2## wherein R.sub.1 is a C.sub.1 -C.sub.4 alkyl or a phenyl group, R and R.sub.3 are as defined above, a compound of formula (III) ##STR3## wherein R.sub.2 is as defined above and X is a cation or a silicon-containing residue, and a salt of a group IIa, IIb or transition element. The compounds of formula (I) are intermediates in the synthesis of penem antibiotics.Type: GrantFiled: April 30, 1993Date of Patent: March 21, 1995Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Walter Cabri, Ilaria Candiani, Franco Zarini, Angelo Bedeschi
-
Patent number: 5382669Abstract: The invention provides a process for the preparation of ergoline derivatives of the formula I ##STR1## the process comprising reacting an ergoline amide of the formula II with an isocyanate of formula III ##STR2## in presence of a metal catalyst and of a phosphorus compound. The compounds of the formula I are useful antiprolactinic and antiparkinson agents.Type: GrantFiled: March 9, 1993Date of Patent: January 17, 1995Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Ilaria Candiani, Walter Cabri, Angelo Bedeschi, Franco Zarini
-
Patent number: 5362740Abstract: A compound of formula (I) ##STR1## wherein R' is hydrogen or methyl, m is zero or 1 and the symbol means that the azabicyclic rings may be in the .alpha. or the .beta. orientation, and the pharmaceutically acceptable salts thereof, are useful in treating CNS disorders, gut motility disorders, and/or emesis and/or pain in mammals, and/or migraine.Type: GrantFiled: November 30, 1992Date of Patent: November 8, 1994Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Angelo Bedeschi, Walter Cabri, Ilaria Candiani, Silvia De Bernardinis, Marcello Marchi, Mario Varasi
-
Patent number: 5304641Abstract: The present invention relates to a process for the preparation of exomethylene cephams, which are useful intermediates in the production of many useful .beta.-lactam antibiotics.More particularly there is provided a process for preparing a compound of formula I ##STR1## wherein n is O or 1, R.sub.1 is hydrogen atom or an organic residue and R.sub.2 is a carboxy protecting group, which process comprises reacting a compound of the formula II ##STR2## wherein X is halogen atom or acetoxy group and R.sub.1 n and R.sub.2 are as defined above with a lanthanide complex.Type: GrantFiled: February 16, 1993Date of Patent: April 19, 1994Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Walter Cabri, Ilaria Candiani, Angelo Bedeschi
-
Patent number: 5286861Abstract: The present invention relates to a novel process for preparing uracil derivatives useful as intermediates in the synthesis of uridines having antiviral or antitumor activity or useful as coadjuvants in antiviral therapy, characterized by converting a compound of the formula II into its mesylate derivative of the formula III which is the reduced to give the desired compound of the formula I: ##STR1## in which R.sub.1 is H, halogen, alkyl, aryl or aralkyl.Type: GrantFiled: August 21, 1992Date of Patent: February 15, 1994Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Angelo Bedeschi, Walter Cabri, Ilaria Candiani, Tiziano Martinengo
-
Patent number: 5180758Abstract: 4-substituted anthracyclinones of general formula (I): ##STR1## wherein R represents a hydrogen atom or a COOR.sub.1 group in which R.sub.1 may be a hydrogen atom or an optionally substituted C.sub.1 -C.sub.10 alkyl group, which are intermediates in the preparation of antitumor anthracycline glycosides, are prepared by:(i)(a) reacting a 4-demethyl-4-sulfonyl-7-deoxy-13-dioxolanyl daunomycinone of formula (V): ##STR2## wherein R' represents an alkyl group having from 1 to 10 carbon atoms optionally substituted by one or more halogen atoms or an aryl group optionally substituted by halogen, alkyl, alkoxy or nitro, in a reducing environment with a catalytic amount of a compound of formula (VIII):ML.sub.n L'.sub.Type: GrantFiled: August 26, 1991Date of Patent: January 19, 1993Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Walter Cabri, Ilaria Candiani, Silvia De Bernardinis, Franco Francalanci