Patents Assigned to Pharmacia & Upjohn S.p.A.
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Patent number: 7037929Abstract: Compounds which are 2-amino-1,3-thiazole derivatives of formula (I) wherein R is a halogen atom, a nitro group, an optionally substituted amino group or it is a group, optionally further substituted, selected from i) straight or branched C1–C8 alkyl, C2–C6 alkenyl or C2–C6 alkynyl; ii) C3–C6 cycloalkyl; iii) aryl or arylalkyl with from 1 to 8 carbon atoms within the straight or branched alkyl chain; R1 is an optionally further substituted group selected from: i) straight or branched C1–C8 alkyl or C2–C6 alkenyl; ii) 3 to 6 membered carbocycle or 5 to 7 membered heterocycle ring; iii) aryl or arylcarbonyl; iv) arylalkyl with from 1 to 8 carbon atoms within the straight or branched alkyl chain; v) arylalkenyl with from 2 to 6 carbon atoms within the straight or branched alkenyl chain; vi) an optionally protected amino acid residue; or a pharmaceutically acceptable salt thereof; are useful for treating cell proliferative disorders associated with an altered cell dependent kinase activity.Type: GrantFiled: October 27, 1999Date of Patent: May 2, 2006Assignee: Pharmacia & Upjohn S.p.A.Inventors: Paolo Pevarello, Raffaella Amici, Gabriella Traquandi, Manuela Villa, Anna Vulpetti, Antonella Isacchi
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Patent number: 7019002Abstract: The invention provides pyrido[2,3-d]pyrimidin-7(8H)-one telomerase inhibitors of the formula where R1, R2 are as defined herein. The invention also provides methods for preparing the compounds of formula I, methods of using the compounds to treat diseases such as cancer, and pharmaceutical compositions comprising the compounds.Type: GrantFiled: December 4, 2002Date of Patent: March 28, 2006Assignee: Pharmacia & Upjohn, S.p.A.Inventors: Mauro Angiolini, Dario Ballinari, Domenico Fusar Bassini, Luisella Bonomini, Markus Gude, Maria Menichincheri, Jurgen Moll, Jean-Yves Trosset
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Patent number: 6863647Abstract: Compounds which are 2-ureido-1,3-thiazole derivatives of formula (I) wherein R is a halogen atom, a nitro group, an optionally substituted amino group or it is a group optionally further substituted, selected from: i) straight or branched C1-C6 alkyl; ii) C3-C6 cycloalkyl; iii) aryl or arylalkyl with from 1 to 6 carbon atoms within the straight or branched alkyl chain; R1 is an optionally substituted group selected from: i) straight or branched C1-C6 alkyl; ii) 3 to 6 membered carbocycle or 5 to 7 membered heterocycle ring; iii) aryl or arylcarbonyl; iv) arylalkyl with from 1 to 6 carbon atoms within the straight or branched alkyl chain; R2 is hydrogen, a straight or branched C1-C6 alkyl or C2-C4 alkenyl or alkynyl group; or, taken together with the nitrogen atom so which they are bonded, R1 and R2 form a substituted or unsubstituted group selected from: i) an optionally benzocondensed or bridged 5 to 7 membered heterocycle; or ii) a 9 to 11 membered spiro-heterocyclic compound; or a pharmaceutically acceptabType: GrantFiled: October 27, 1999Date of Patent: March 8, 2005Assignee: Pharmacia & Upjohn S.p.A.Inventors: Paolo Pevarello, Raffaella Amici, Gabriella Traquandi, Manuela Villa, Anna Vulpetti, Antonella Isacchi
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Patent number: 6794385Abstract: The present invention relates to a class of compounds represented by the formula (I) or a pharmaceutical acceptable salt, prodrug or ester thereof, pharmaceutical compositions comprising compounds of the formula (I), and methods of selectively inhibiting or antagonizing &agr;v&bgr;3 integrin.Type: GrantFiled: August 8, 2001Date of Patent: September 21, 2004Assignee: Pharmacia & Upjohn, S.p.A.Inventors: Paola Vianello, Tiziano Bandiera, Mario Varasi
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Patent number: 6753316Abstract: Compounds which are acryloyl substituted distamycin derivatives of formula (I) wherein: n is 2, 3 or 4; m is 1 or 2; X and Y are the same or different and are selected, independently for each heterocyclic ring of the polyetherocyclic chain, from N and CH; R1 and R2, which are the same or different, are selected from hydrogen, halogen, and C1-C4 alkyl; R3 is hydrogen or halogen; B is selected from (a), (b), (c), (d), (e), (f), (g) and —C≡N; wherein R4, R5, R6, R7, R8, R10, R11, and R12 are, independently from each other, hydrogen or C1-C4 alkyl; and R9 is hydrogen or hydroxy, or pharmaceutically acceptable salt thereof; provided that a) at least one of R4, R5 and R6 is alkyl b) at least one of the heterocyclic rings within the polyheterocyclic chain is other than pyrole; and c) X and Y are not both N for the same heterocyclic ring; are useful as antitumor agents.Type: GrantFiled: September 19, 2000Date of Patent: June 22, 2004Assignee: Pharmacia & Upjohn S.p.A.Inventors: Paolo Cozzi, Pier Giovanni Baraldi, Italo Beria, Marina Caldarelli, Laura Capolongo, Romeo Romagnoli
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Patent number: 6750215Abstract: The present invention relates to a class of compounds represented by the formula (I) or a pharmaceutical acceptable salt, prodrug or ester thereof, pharmaceutical compositions comprising compounds of the formula (I), and methods of selectively inhibiting or antagonizing &agr;v&bgr;3 integrin.Type: GrantFiled: August 8, 2001Date of Patent: June 15, 2004Assignee: Pharmacia & Upjohn, S.p.A.Inventors: Paola Vianello, Tiziano Bandiera
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Patent number: 6593303Abstract: There are provided the combined use of 4-demethoxy-3′-deamino-3′-aziridinyl-4′-methansulfonyl daunorubicin or 4-demethoxy-N,N-bis(2-chloroethyl)-4′-methansulfonyl daunorubicin and an anti-neoplastic anti-mitotic compound and/or a platinum derivative in the treatment of tumors, as well as in the prevention or treatment of metastasis or in the treatment of tumors by inhibition of angiogenesis.Type: GrantFiled: August 22, 2001Date of Patent: July 15, 2003Assignee: Pharmacia & Upjohn, S.p.A.Inventors: Cristina Geroni, Marina Ripamonti, Michele Caruso, Antonino Suarato
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Patent number: 6562562Abstract: A surgical procedure (partial hepatectomy) in the nonhuman primate allows repeated removal of large liver tissue samples from a single animal for the preparation of liver tissue slices and primary cell culture of hepatocytes. The open biopsy procedure, alternating non-anatomic and anatomic partial liver resection monthly on the same liver lobe, follows a surgical protocol allowing animal welfare, survival, and multiple sampling (at least 8) from the same animal, thus reducing considerably the number of animals needed for research purposes.Type: GrantFiled: March 2, 2001Date of Patent: May 13, 2003Assignee: Pharmacia & Upjohn S.p.A.Inventors: Francesco Casu', Claudio Bernardi, Luciano Dho, Bruno Rosa
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Publication number: 20030087839Abstract: The present invention relates to combined preparations comprising a morpholinyl anthracycline administered in combination anticancer agents chosen from an allylating agent, an antimetabolite, a topoisomerase II inihbitor, a topoisomerase I inhibitor, an antimitotic drug and a platinum derivative, which are useful anticancer therapy, particularly in the treatment of a primary or metastatic liver cancer.Type: ApplicationFiled: October 31, 2002Publication date: May 8, 2003Applicant: PHARMACIA & UPJOHN S.p.AInventors: Maria Christina Geroni, Marina Ripamonti, Michele Caruso, Antonino Suarato
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Publication number: 20030073692Abstract: Compounds which are amino-phthalazinone derivatives and pharmaceutically acceptable salts thereof, together with pharmaceutical compositions comprising them are disclosed; these compounds or compositions are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, cell proliferative disorders, Alzheimer's disease, viral infections, auto-immune diseases and neurodegenerative disorders.Type: ApplicationFiled: August 7, 2001Publication date: April 17, 2003Applicant: PHARMACIA & UPJOHN S.p.A.Inventor: Maurizio Pulici
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Publication number: 20030023031Abstract: According to the invention, there is provided a method of manufacturing a medicament for use in the treatment of cancer or viral infections which comprises obtaining a cancer treating effective amount of a compound of formula (I), 1Type: ApplicationFiled: July 17, 2002Publication date: January 30, 2003Applicant: Pharmacia & Upjohn S.p.A.Inventors: Paolo Cozzi, Italo Beria, Giovanni Biasoli, Marina Caldarelli, Laura Capolongo, Cristina Franzetti
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Patent number: 6482827Abstract: A compound, which is an amine derivative of formula (I) wherein W is —CNHOH or —COOH: R1 and R2 are each hydrogen or an organic residue, R3 is an organic group, Q is a secondary or tertiary acyclic or cyclic amido group, and the pharmaceutically acceptable salts, solvates and hydrates thereof, are inhibitors of matrix metalloproteinases (MMPs) and of the release of tumor necrosis factor-alpha (TNF) from cells. They are therefore useful in the prevention, control and treatment of diseases in which MMPs or TNF are involved, especially tumoral and inflammatory diseases. Processes for their preparation and pharmaceutical compositions containing them are also described.Type: GrantFiled: March 10, 1999Date of Patent: November 19, 2002Assignee: Pharmacia & Upjohn S.p.A.Inventors: Marco Alpegiani, Pierluigi Bissolino, Francesca Abrate, Ettore Perrone, Riccardo Corigli, Daniela Jabes
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Patent number: 6458768Abstract: Compounds which are benzoheterocyclic distamycin derivatives of formula (I), wherein n is 2, 3 or 4; A is a heteroatom selected from O and S or is a group NR, wherein R is hydrogen or C1-C4 alkyl; B is CH or N; R1 is hydrogen or C1-C4 alkyl; G is selected from the group consisting of (a, b, c, d, e, f, g, h, i, j), and —C≡N; wherein R5, R6, R7, R8, R9, R10, R11 and R12 are, independently from each other, hydrogen or C1-C4 alkyl; T is a group of formula (II) or (III) as defined above, wherein p is 0 or 1; R2 and R3 are, independently from each other, hydrogen, C1-C4 alkyl optionally substituted by one or more fluorine atoms, or C1-C4 alkoxy; R4 is C1-C4 alkyl or C1-C3 haloalkyl; X1 and X2 are halogen atoms or pharmaceutically acceptable salts thereof; provided that at least one of R5, R6 and R7 is alkyl; are useful as antitumor agents.Type: GrantFiled: September 19, 2000Date of Patent: October 1, 2002Assignee: Pharmacia & Upjohn, S.p.A.Inventors: Paolo Cozzi, Pier Giovanni Baraldi, Italo Beria, Marina Caldarelli, Laura Capolongo, Romeo Romagnoli
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Patent number: 6420379Abstract: 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: November 20, 2000Date of Patent: July 16, 2002Assignee: Pharmacia & Upjohn S.p.A.Inventors: Ilaria Candiani, Angelo Bedeschi, Giuseppina Visentin, Maria Chiara Fagnola, Laura Capolongo
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Patent number: 6414013Abstract: Compounds which are 3-aminocarbonyl-2-carboxamido-thiophene derivatives of formula (I): wherein R1 and R2 are, independently from each other, hydrogen, halogen or an optionally substituted group selected from aryl, straight or branched C1-C6 alkyl or aryl C1-C6 alkyl; or, taken together with the thiophene bond to which they are linked, R1 and R2 form a —(CH2)m—(NR4)n—(CH2)p— group wherein m and p are, each independently, an integer form 1 to 3, n is 0 or 1 and m+n+p is an integer from 3 to 5; and R4 is hydrogen or an optionally substituted straight or branched C1-C6 alkyl group; R3 is a group, optionally further substituted, selected from: i) straight or branched C1-C8 alkyl, C2-C6 alkenyl, C2-C6 alkynyl or C2-C6 alkylcarbonyl; ii) aryl; iii) 3 to 7 membered carbocycle; iv) 5 to 7 membered heterocycle with from 1 to 3 heteroatoms selected from nitrogen, oxygen and sulphur; or a pharmaceutically acceptable salt thereof; are useful in the treatment of diseasesType: GrantFiled: June 19, 2000Date of Patent: July 2, 2002Assignee: Pharmacia & Upjohn S.p.A.Inventors: Daniele Fancelli, Paolo Pevarello, Mario Varasi
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Patent number: 6407122Abstract: The present invention relates to amino-benzothiazole compounds of formula (I) wherein X, Y, Z and R1 are as defined in the specification, their pharmaceutically acceptable salts, processes for their preparation, pharmaceutical composition comprising such compounds and their use as neuroprotective agents.Type: GrantFiled: June 1, 2000Date of Patent: June 18, 2002Assignee: Pharmacia & Upjohn S.p.A.Inventors: Sergio Mantegani, Paolo Cremonesi, Mario Varasi, Carmela Speciale
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Patent number: 6403563Abstract: The combination of 4-demethoxy-3′-deamino-3′-aziridinyl-4′-methansulfonyl daunorubicin or 4-demethoxy-N,N-bis(2-chloroethyl)-4′-methansulfonyl daunorubicin together with an antineoplastic topoisomerase I inhibitor yields preparations exhibiting anti-cancer effects. These preparations can be used in the treatment of tumors and especially 4-demethoxy-3′-deamino-3′-aziridinyl-4′-methansulfonyl daunorubicin in the treatment of brain tumors.Type: GrantFiled: September 20, 2000Date of Patent: June 11, 2002Assignee: Pharmacia & Upjohn S.p.A.Inventors: Cristina Geroni, Marina Ripamonti, Michele Caruso, Antonino Suarato
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Patent number: 6403603Abstract: 9-Amino-20(S)-camptothecin (I) is prepared by reducing 12-nitro-20(S)-camptothecin (II); converting the resulting 12-amino-20(S)-camptothecin (III) into a compound of formula (IV) wherein X is a group which can be reductively removed; reacting the compound of formula (IV) with a nitrating agent, to obtain thereby the corresponding 9-nitro-20(S)-camptothecin compound of formula (V) substituted at the 12-position by the group X; reducing in a single step the compound of formula (V), so obtaining the 9-amino-20(S)-camptothecin of formula (I); or reducing the compound of formula (V), so obtaining the corresponding 9-amino-20(S)-camptothecin compound of formula (VI) substituted at the 12-position by the group X and reductively removing the X group from the compound of formula (VI), so obtaining 9-amino-20(S)-camptothecin.Type: GrantFiled: August 2, 1994Date of Patent: June 11, 2002Assignee: Pharmacia & Upjohn S.p.A.Inventors: Angelo Bedeschi, Walter Cabri, Ilaria Candiani, Franco Zarini
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Patent number: 6387900Abstract: 3-ureido-pyrazole derivatives represented by formula (I): where R, R1 and R2 are as described herein, or pharmnaceutically acceptable salts thereof; are useful, for example, for the treatment of cancer, cell proliferative disorders, Alzheimer's disease, viral infections, auto-immune diseases or neurodegenerative diseases.Type: GrantFiled: August 12, 1999Date of Patent: May 14, 2002Assignees: 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
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Patent number: 6376617Abstract: Water soluble polymeric conjugates of camptothecin consist essentially of N-(2-hydroxypropyl)methacryloylamide units linked via a spacer group to a residue of a camptothecin such as irinotecan or its non-soluble metabolite, 7-ethyl-10-hydroxy-camptothecin. The conjugates possess enhance antitumor activity and decreased toxicity with respect to the free drug. A process for their preparation and the pharmaceutical compositions containing them are also described.Type: GrantFiled: June 3, 1999Date of Patent: April 23, 2002Assignee: Pharmacia & Upjohn S.p.A.Inventors: Francesco Angelucci, Gabriele Fachin, Valeria Caiolfa, Antonino Suarato