Patents Assigned to Pharmacia & Upjohn S.p.A.
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Patent number: 6369096Abstract: A compound, having utility as an immunomodulating agent, which is a prodigiosine of formula (I): wherein R1 is hydrogen or C1-C5 alkyl; and R2 is a C1-C5 alkyl; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: October 7, 1999Date of Patent: April 9, 2002Assignee: Pharmacia & Upjohn S.p.A.Inventors: Roberto D'Alessio, Ermes Vanotti, Alberto Bargiotti, Marcellino Tibolla, Mario Ferrari, Anna Maria Isetta, Francesco Colotta
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Patent number: 6335342Abstract: Novel 1H-pyrrolo[2,3-b]pyridines which are represented by formula (I): wherein R is a hydrogen or halogen atom or a group selected from —CN, —OH, —OCOR4, —(CH2)nNH2, —(CH2)nNHR4, —(CH2)nNHCOR4, —(CH2)nNHCONR4R5, —(CH2)nNHCOOR4, or —(CH2)nNHSO2R4, wherein n is either 0 or 1, R4 and R5 are as described in the specification; R1 is hydrogen or an optionally substituted alkyl group; R2 is an optionally substituted group selected from alkyl or aryl; R3 is hydrogen or a group selected from —CONR4R5, —COOR4, —CONHOR4, —SO2NHR4, alkylsulphonylaminocarbonyl or perfluorinated alkylsulphonylaminocarbonyl; or a pharmaceutically acceptable salt thereof, are disclosed. These compounds are useful for treating cell proliferative disorders associated with an altered cell dependent kinase activity.Type: GrantFiled: June 19, 2000Date of Patent: January 1, 2002Assignee: Pharmacia & UpJohn S.p.A.Inventors: Antonio Longo, Maria Gabriella Brasca, Paolo Orsini, Gabriella Traquandi, Valeria Pittalà, Anna Vulpetti, Mario Varasi, Paolo Pevarello
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Patent number: 6328953Abstract: The invention relates to polymeric conjugates of 20-O-[glycyl-aminoacyl-glycyl]-camptothecins and a process for producing the same.Type: GrantFiled: March 31, 2000Date of Patent: December 11, 2001Assignee: Pharmacia & Upjohn S.p.A.Inventors: Francesco Angelucci, Fabrizio Orzi, Gabriele Fachin, Valeria Caiolfa, Moreno Zamai, Antonino Suarato
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Patent number: 6323240Abstract: 4-phenyl-4-oxo-butanoic acid derivatives for use in the treatment of the human or animal body by therepy; particularly as kynurenine-3-hydroxylase inhibitors, in the prevention and/or treatment of a neurodegenerative disease wherein the inhibition of such an enyzme is needed. The present invention further comprises a selected class of the above mentioned 4-phenyl-4-oxo-butanoic acid derivatives, their pharmaceutically acceptable salts, a process for their preparation and pharmaceutical compositions containing them.Type: GrantFiled: May 1, 1998Date of Patent: November 27, 2001Assignee: Pharmacia & Upjohn S.p.A.Inventors: Antonio Giordani, Paolo Pevarello, Carmela Speciale, Mario Varasi
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Patent number: 6316451Abstract: A compound of formula (1) wherein R1 is hydrogen, hydroxy, a group of formula OR5 wherein R5 is C1-C6 alkyl, C2-C6 alkenyl or C3-C8 cycloalkyl, halogen, amino which may be unsubstituted or mono or disubstituted by C1-C6 alkyl, C2-C6 alkenyl, aralkyl, acyl or trifluoroacetyl; R2 is hydrogen, hydroxy, a group NR6R7 wherein R6 and R7 independently represent hydrogen, an optionally substituted C1-C6 alkyl, C2-C6 alkenyl, C3-C8 cycloalkyl or, taken together with the nitrogen atom, represent an optionally substituted C3-C8 heterocyclic ring; R3 is hydrogen, hydroxy, R4 is a 2-substituted thiazolyl or imidazolyl system and the pharmaceutically acceptable salt thereof, is useful in the treatment of amyloidosis. Processes for the preparation and pharmaceutical compositions are also described.Type: GrantFiled: September 26, 2000Date of Patent: November 13, 2001Assignee: Pharmacia & Upjohn S.p.A.Inventors: Sergio Mantegani, Gabriella Traquandi, Tiziano Bandiera, Jacqueline Lansen, Mario Varasi
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Patent number: 6284896Abstract: There are provided compounds of formula (I), wherein R1 is a hydrogen, chlorine or bromine atom or a methyl, methylthio, hydroxy, cyano or carboxamido group; R2 is C1-C3 alkyl or an alkyl group; R3 and R4 are independently a hydrogen atom, a C1-C5 alkyl group, a C3-C5 alkenyl group, a C5-C6 cycloalkyl C1-C3 alkyl group, a phenyl-C3-C5 alkenyl or phenyl group: which groups are optionally substituted by C1-C3 alkyl, C1-C3 alkoxy, triflouromethyl, hydroxy or amino group; or a group of formula (a), wherein R6 is hydrogen atom or a C1-C3 alkyl group and R7 is a phenyl group, a substituted phenyl group as described above or a heterocyclic ring, R5 is a hydrogen or bromine atom or an organic residue and R is H or an organic residue, or a pharmaceutically acceptable salt thereof. A process for their preparation and the pharmaceutical compositions comprising them are also provided.Type: GrantFiled: December 29, 1997Date of Patent: September 4, 2001Assignee: Pharmacia & Upjohn S.p.A.Inventors: Sergio Mantegani, Tiziano Bandiera, Enzo Brambilla, Carla Caccia, Nicola Carfagna
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Patent number: 6258786Abstract: The present invention relates to anthracycline glycosides, to a process for their preparation and to pharmaceutical compositions containing the same.Type: GrantFiled: December 13, 1999Date of Patent: July 10, 2001Assignee: Pharmacia & Upjohn S.p.A.Inventors: Maria Cristina Geroni, Marina Ripamonti, Michele Caruso, Antonino Suarato
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Patent number: 6245358Abstract: A lyophilized composition comprising (a) a conjugate comprising a N-alkyl methacrylamide-based copolymer and an anthracycline glycoside linked through a peptide spacer to the copolymer and (b) a cosolubilizing agent may optionally also contain (c) a filler. Also optionally, a targeting moiety may be linked to the copolymer of the conjugate via a peptide spacer. An injectable solution of the conjugate is obtained by reconstitution of the lyophilized composition.Type: GrantFiled: December 28, 1992Date of Patent: June 12, 2001Assignee: Pharmacia & Upjohn S.p.A.Inventors: Marco Adami, Roberto Magrini, Paolo Maranghi, Antonino Suarato
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Patent number: 6245742Abstract: The present invention relates to peptides and peptidomimetic compounds and pharmaceutical compositions containing them as useful pharmacological agents in the control or treatment of proliferative diseases such as cancer, against tumor growing and/or tumoral metastasis, and psoriasis and in the control or treatment of inflammatory, allergic, autoimmune, viral, and cardiovascular diseases. These new compounds have the unique property to inhibit the recognition of several phosphotyrosine containing motifs within all the cellular receptors and cytosolic transducers by a wide spectrum of SH2 domains contained in cytosolic transducers and other effector proteins laying along different pathways of the signal transduction process and with a particularly high affinity for the SH2 domain of the adaptor transducer Grb2, a key element along the pathway to mitogenesis and motogenesis, this last activity leading to invasiveness and to metastasis.Type: GrantFiled: October 15, 1997Date of Patent: June 12, 2001Assignee: Pharmacia & Upjohn S.p.A.Inventors: Carlo Battistini, Patrizia Giordano, Sabrina De Rosa, Fabio Corradi, Paolo Comoglio, Alberto Bardelli
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Patent number: 6218418Abstract: 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: GrantFiled: September 22, 2000Date of Patent: April 17, 2001Assignees: 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
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Patent number: 6214860Abstract: A pharmaceutical composition for use in antineoplastic therapy in mammals, including humans, comprising a biologically active ureido compound of formula (I) wherein each of m and n, being the same, is an integer of 1 to 3; and each of the R groups, which are the same, is a naphthyl group substituted by 1 to 3 sulfonic groups, or a pharmaceutically acceptable salt thereof, and an antineoplastic agent selected from the group consisting of an antineoplastic vinca alkaloid, an antineoplastic antibiotic, an antineoplastic antimetabolite, an antineoplastic platinum coordination complex, an antineoplastic taxane compound, an antineoplastic ceramide compound, an antineoplastic distamycin compound, an antineoplastic epidophyllotoxin compound and an antineoplastic topoisomerase I inhibitor, and a pharmaceutically acceptable carrier or excipient, in amounts effective to produce a synergistic antineoplastic effect, is provided herein.Type: GrantFiled: August 30, 1999Date of Patent: April 10, 2001Assignee: Pharmacia & Upjohn S.p.A.Inventors: Francesco Sola, Maria Grandi
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Patent number: 6211192Abstract: The present invention relates to alkynyl-substituted camptothecins of formula (I) wherein X, R1, R2 are as defined herein, and the pharmaceutically salts thereof. These compounds are useful in therapy as antitumor agents.Type: GrantFiled: August 12, 1999Date of Patent: April 3, 2001Assignee: Pharmacia & Upjohn S.p.A.Inventors: Ilaria Candiani, Angelo Bedeschi, Giuseppina Visentin, Maria Chiara Fagnola, Laura Capolongo
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Patent number: 6210930Abstract: The present invention is directed to a process for improving daunorubicin and doxorubicin production by means of a recombinant microorganism in which a gene of daunorubicin metabolism is mutated. The mutated gene is preferably dnrU and/or dnrX.Type: GrantFiled: January 14, 1999Date of Patent: April 3, 2001Assignee: Pharmacia & Upjohn, S.P.A.Inventors: Silvia Filippini, Natalia Lomovskaya, Leonid Fonstein, Anna Luisa Colombo, C. Richard Hutchinson, Sharee L. Otten, Umberto Breme
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Patent number: 6207709Abstract: 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: GrantFiled: February 24, 1999Date of Patent: March 27, 2001Assignee: Pharmacia & Upjohn S.p.A.Inventors: Mario Varasi, Antonio Giordani, Massimo Cini, Carmela Speciale, Alberto Bianchetti
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Patent number: 6194451Abstract: A compound of formula (I), wherein W is —NHOH or —OH, R1 is either free or protected hydroxymethyl or mercaptomethyl or derivatives thereof, R2 is free or protected hydroxy, R3 and R4 is an organic group, R5 is hydrogen or methyl, or R4 and R5, together with the nitrogen atom to which they are attached, constitute an azaheterocyclyl group, and the solvates, hydrates and pharmaceutically acceptable salts thereof, can inhibit matrix metalloproteinases and the release of tumour necrosis factor (TNF). Processes for producing the compound, intermediates involved in the processes, and pharmaceutical compositions containing the compound are also described.Type: GrantFiled: July 30, 1999Date of Patent: February 27, 2001Assignee: Pharmacia & Upjohn S.p.A.Inventors: Marco Alpegiani, Massimiliano Palladino, Riccardo Corigli, Daniela Jabes, Ettore Perrone, Maria Francesca Abrate, Pierluigi Bissolino, Marina Lombroso
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Patent number: 6187758Abstract: An anthracycline glycoside of formula I wherein R is one of the two following residues: or a pharmaceutically acceptable salt thereof.Type: GrantFiled: August 27, 1999Date of Patent: February 13, 2001Assignee: Pharmacia & Upjohn S.p.A.Inventors: Cinzia Portello, Emanuele Arlandini, Umberto Breme, Anna Luisa Colombo, Giuliano Franchi, Giuliano Oronzo, Marco Tató, Luisa Garofano, Marina Ciomei
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Patent number: 6177408Abstract: A compound which is a distamycin derivative of formula (I), wherein n is 2, 3 or 4; R0is C1-C4 alkyl or C1-C3 haloalkyl; R1 and R2, which may be the same or different, are each hydrogen, C1-C4 alkyl optionally substituted by one or more fluorine atoms, or C1-C4 alkoxy; X is a halogen atom; B is selected from (A, B, C, D, E, F, G, H, I, J and K); wherein R3, R4, R5, R6, R7, R8, and R9, which may be the same or different, are each hydrogen or C1-C4 alkyl, and m is 0, 1, or 2; or a pharmaceutically acceptable salt thereof. Such compounds are useful as antineoplastic and antiviral agents.Type: GrantFiled: November 13, 1998Date of Patent: January 23, 2001Assignee: Pharmacia & Upjohn S.p.A.Inventors: Paolo Cozzi, Italo Beria, Marina Caldarelli, Maria Cristina Geroni, Enrico Pesenti
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Patent number: 6165980Abstract: A distamycin derivative of formula (I): ##STR1## wherein: n is 2, 3 or 4;R.sub.0 is C.sub.1 -C.sub.4 alkyl or --CH.sub.2 CH.sub.2 --X.sub.2, wherein X.sub.2 is a halogen atom;R.sub.1 and R.sub.2 are selected, each independently, from: hydrogen, C.sub.1 -C.sub.4 alkyl optionally substituted by one or more fluorine atoms, C.sub.1 -C.sub.4 alkoxy, and halogen;X.sub.1 is a halogen atom;B is selected from: ##STR2## wherein R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, and R.sub.9 are, each independently, hydrogen or C.sub.1 -C.sub.4 alkyl, and m is 0, 1 or 2; with the proviso that, when R.sub.0 is --CH.sub.2 CH.sub.2 --X.sub.2, B is different from --(CH.sub.2).sub.m --NR.sub.6 R.sub.7 and at least one of R.sub.3, R.sub.4, and R.sub.5 is C.sub.1 -C.sub.4 alkyl;or a pharmaceutically acceptable salt thereof.Type: GrantFiled: July 17, 1998Date of Patent: December 26, 2000Assignee: Pharmacia & Upjohn S.p.A.Inventors: Paolo Cozzi, Italo Beria, Marina Caldarelli, Maria Cristina Geroni, Enrico Pesenti
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Patent number: 6153642Abstract: Benzoheterocyclic distamycin derivatives of formula (I) wherein: n is 2, 3 or 4; A is O, S, or NR, wherein R is hydrogen or C.sub.1 -C.sub.4 alkyl; B is CH or N; R.sub.1 is hydrogen or C.sub.1 -C.sub.4 alkyl; T is selected from; (i) formula (II) wherein: p is zero or 1; R.sub.2 and R.sub.3 are selected, each independently, from: hydrogen, C.sub.1 -C.sub.4 alkyl optionally substituted by one or more fluorine atoms, and C.sub.1 -C.sub.4 alkoxy; R.sub.4 is C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.3 haloalkyl; X.sub.1 is a halogen atom; and (ii) formula (III) wherein X.sub.2 is a halogen atom; and pharmaceutically acceptable salts thereof, are described. Such compounds are useful as antineoplastic and antiviral agents.Type: GrantFiled: May 4, 1999Date of Patent: November 28, 2000Assignee: Pharmacia & Upjohn S.p.A.Inventors: Paolo Cozzi, Pier Giovanni Baraldi, Italo Beria, Marina Caldarelli, Laura Capolongo, Giampiero Spalluto, Romeo Romagnoli
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Patent number: 6147073Abstract: A tetralylmethylene-2-oxindole derivative having the following formula (I) ##STR1## wherein one or two of R, R.sub.1, R.sub.2 and R.sub.3 the said two being the same or different, are selected from:a) --X--(CH.sub.2).sub.m --NH.sub.2, --X--(CH.sub.2).sub.m --NR.sub.4 R.sub.5 or --X--(CH.sub.2).sub.m --NHR.sub.6, in which X is --O--, --S-- or --NH--, m is an integer of 2 to 4, one of R.sub.4 and R.sub.5 is hydrogen or C.sub.1 -C.sub.6 alkyl and the other is C.sub.1 -C.sub.6 alkyl or R.sub.4 and R.sub.5 taken together with the N atom to which they are linked form a 5 to 7 membered saturated heteromonocycle, and R.sub.6 is C.sub.2 -C.sub.6 alkanoyl or a C-terminally linked peptidyl residue containing from 1 to 3 aminoacids wherein the terminal amino group is either free or protected or in an alkylated form to provide a --NR.sub.4 R.sub.5 group in which R.sub.4 and R.sub.5 are as defined above.Type: GrantFiled: January 12, 1998Date of Patent: November 14, 2000Assignee: Pharmacia & Upjohn S.p.A.Inventors: Carlo Battistini, Antonella Ermoli, Sergio Vioglio, Franco Buzzetti, Dario Ballinari