Patents by Inventor Francesco Angelucci
Francesco Angelucci 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: 8106069Abstract: Compounds which are pyrrolo[2,3-b]pyridine derivatives or pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds 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; also disclosed is a process under SPS conditions for preparing the compounds of the invention and chemical libraries comprising a plurality of them.Type: GrantFiled: April 23, 2010Date of Patent: January 31, 2012Assignee: Pfizer Italia S.r.l.Inventors: Barbara Salom, Matteo D'Anello, Maria Gabriella Brasca, Patrizia Giordano, Katia Martina, Francesco Angelucci, Frederick Arthur Brookfield, William John Trigg, Edward Andrew Boyd, Jonathan Anthony Larard
-
Publication number: 20100210476Abstract: Compounds which are pyrrolo[2,3-b]pyridine derivatives or pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds 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; also disclosed is a process under SPS conditions for preparing the compounds of the invention and chemical libraries comprising a plurality of them.Type: ApplicationFiled: April 23, 2010Publication date: August 19, 2010Applicant: PFIZER ITALIA S.R.L.Inventors: Barbara Salom, Matteo D'Anello, Maria Gabriella Brasca, Patrizia Giordano, Katia Martina, Francesco Angelucci, Frederick Arthur Brookfield, William John Trigg, Edward Andrew Boyd, Jonathan Anthony Larard
-
Patent number: 7728140Abstract: Compounds which are pyrrolo[2,3-b]pyridine derivatives or pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds 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; also disclosed is a process under SPS conditions for preparing the compounds of the invention and chemical libraries comprising a plurality of them.Type: GrantFiled: December 23, 2004Date of Patent: June 1, 2010Assignee: Pfizer Italia S.r.l.Inventors: Barbara Salom, Matteo D'Anello, Maria Gabriella Brasca, Patrizia Giordano, Katia Martina, Francesco Angelucci, Frederick Arthur Brookfield, William John Trigg, Edward Andrew Boyd, Jonathan Anthony Larard
-
Patent number: 7371862Abstract: The present invention is directed to compounds of the formula or pharmaceutically acceptable salts, prodrug, solvate or optical isomer thereof, pharmaceutical compositions containing same and use thereof for treating diseases linked to disregulated cell proliferation or to disregulated protein kinase.Type: GrantFiled: November 11, 2005Date of Patent: May 13, 2008Assignee: Pfizer Italia S.r.l.Inventors: Ermes Vanotti, Francesco Angelucci, Alberto Bargiotti, Maria Gabriella Brasca, Antonella Ermoli, Maria Menichincheri
-
Publication number: 20070112020Abstract: The present invention is directed to compounds of the formula or pharmaceutically acceptable salts, prodrug, solvate or optical isomer thereof, pharmaceutical compositions containing same and use thereof for treating diseases linked to disregulated cell proliferation or to disregulated protein kinase.Type: ApplicationFiled: November 11, 2005Publication date: May 17, 2007Applicant: Pharmacia Italia S.p.A.Inventors: Ermes Vanotti, Francesco Angelucci, Alberto Bargiotti, Maria Brasca, Antonella Ermoli, Maria Menichincheri
-
Publication number: 20050256151Abstract: Compounds which are pyrrolo[2,3-b]pyridine derivatives or pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds 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; also disclosed is a process under SPS conditions for preparing the compounds of the invention and chemical libraries comprising a plurality of them.Type: ApplicationFiled: December 23, 2004Publication date: November 17, 2005Applicant: Pharmacia Italia S.p.A.Inventors: Barbara Salom, Matteo D'Anello, Maria Brasca, Patrizia Giordano, Katia Martina, Francesco Angelucci, Frederick Brookfield, William Trigg, Edward Boyd, Jonathan Larard
-
Publication number: 20050107543Abstract: The present invention provides compounds or formula (1) R1—HN—CH2—CF2—(CH2)l—CR3R4—CO—R2, wherein: l is 0, 1 or 2, R1 is a labile amino protecting group, R2 is hydroxy group or the residue or an activated ester or halogen atom; R3 and R4 are independently hydrogen atom or C1-C4 alkyl chain. There are also provided their preparation and the water-soluble conjugates based on these linkers, endowed with selective anticancer activity.Type: ApplicationFiled: July 29, 2002Publication date: May 19, 2005Inventors: Francesco Angelucci, Antonino Suarato, Michele Caruso, Alessandra Scolaro, Enrico Pesenti, Daniela Faiardi
-
Publication number: 20030195152Abstract: Water soluble polymeric conjugates of antitumor agents of formula (A) P-[W2]p-S0-[W1]r-[D] wherein: P is a water soluble polymer; [W1] is a residue of formula —HN-Z1-CO— in which Z1 represents a linear or branched C2-C12 alkylene chain or the residue of formula —C6HC—CH2—O—; [W2] is a residue of formula —HN-Z2-CO— in which Z2 represents a C2-C12 linear or branched alkylene chain; p and r are 0 or 1; S0 is a peptide that selectively is cleaved at the tumor site mainly by the action of the matrix metalloproteinases gelatinase; [D] is the residue of an antitumor agent. The conjugates possess enhanced antitumor activity and decreased toxicity with respect to the free drug. A process for their preparation, useful intermediates and pharmaceutical compositions containing them are also described.Type: ApplicationFiled: April 10, 2003Publication date: October 16, 2003Inventors: Antonio Suarato, Francesco Angelucci, Michele Caruso, Alessandro Scolaro, Daniele Volpi, Moreno Zamai
-
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
-
Publication number: 20020032331Abstract: 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 amptothecin. 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: ApplicationFiled: June 3, 1999Publication date: March 14, 2002Inventors: FRANCESCO ANGELUCCI, GABRIELE FACHIN, VALERIA CAIOLFA, ANTONINO SUARATO
-
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
-
Patent number: 5776458Abstract: The present invention provides anthracycline conjugates with carriers such as monoclonal polyclonal antibodies, proteins or peptides, or other synthetic carriers. These anthracycline conjugates provide pharmaceutical compositions which are useful for treating certain mammalian tumors. The compounds of the present invention have higher potency than anthracyclines, and improved therapeutic efficacy and reduced toxic effects.Type: GrantFiled: March 27, 1995Date of Patent: July 7, 1998Assignee: Pharmacia & Upjohn S.p.A.Inventors: Francesco Angelucci, Daniela Ruggieri, Stefania Stefanelli, Antonino Suarato, Laura Bersani
-
Patent number: 5773522Abstract: A polymeric conjugate consists essentially of: (i) from 60 to 99 mol % of N-(2-hydroxypropyl) methacryloylamide units represented by formula 1: ##STR1## (ii) from 1 to 40 mol % of 20-0-(N-methacryloylglycyl-aminoacyl) camptothecin units represented by formula 2 ##STR2## wherein ?A! is a spacer group having respective terminal amino and carbonyl groups which are separated by at least three atoms and O-CPT represents a residue of a camptothecin, the C-20 hydroxy group of the camptothecin being linked to the terminal carbonyl group of the spacer group ?A!; and (iii) from 0 to 10 mol % of N-methacryloylglycine or N-(2-hydroxy-propyl)methacryloylglycinamide units represented by formula 3: ##STR3## wherein Z represents hydroxy or a residue of formula --NH--CH.sub.2 --CH(OH)--CH.sub.3.Type: GrantFiled: June 8, 1995Date of Patent: June 30, 1998Assignee: Pharmacia S.p.A.Inventors: Francesco Angelucci, Antonino Suarato
-
Patent number: 5719265Abstract: A polymer conjugate consisting essentially of: from 90 to 99.9 mol % of units represented by the formula ##STR1## from 0.1 to 5 mol % of units represented by the formula ##STR2## wherein one of R.sub.1 and R.sub.2 is a copolymer residue of the formula ##STR3## and the other one is hydrogen atom; from 0 to 9.Type: GrantFiled: July 27, 1995Date of Patent: February 17, 1998Assignee: Pharmacia & Upjohn S.P.A.Inventors: Nicola Mongelli, Francesco Angelucci, Enrico Pesenti, Antonino Suarato, Giovanni Biasoli
-
Patent number: 5571785Abstract: The present invention provides polymer-bound anthracyclines of formula A which consists essentially of three units represented by formulae 1, 2 and 3: ##STR1## wherein: Gly represents glycine;n is 0 or 1;x is from 70 to 98 mol %,y is from 1 to 29 mol %,z is from 1 to 29 mol %,R.sub.1 is a C.sub.1 -C.sub.6 alkyl group substituted by one or more hydroxy groups;Y is an amino acid residue or a peptide spacer;[NH--D] is the residue of an anthracycline aminoglycoside [NH.sub.2 --D]; andZ is a hydroxy group or a residue of formula --NHR.sub.1 wherein R.sub.1 is as defined above. Methods for their preparation and pharmaceutical compositions containing them are also provided.Type: GrantFiled: December 20, 1994Date of Patent: November 5, 1996Assignee: Farmitalia Carlo Erba S.r.lInventors: Francesco Angelucci, Maria Grandi, Antonino Suarato
-
Patent number: 5569720Abstract: A polymer conjugate consisting essentially of: from 90 to 99.9 mol % of units represented by the formula ##STR1## from 0.1 to 5 mol % of units represented by the formula ##STR2## wherein one of R.sub.1 and R.sub.2 is a copolymer residue of the formula ##STR3## and the other one is hydrogen atom; from 0 to 9.9 mol % of units represented by the formula ##STR4## wherein R is a phenyl or t-butoxy group, R.sub.3 is H or an acetyl group, A and A.sub.1 which may be the same or different, represent a chemical single bond, an amino acid residue or peptide spacer selected from .beta. Ala, Gly, Phe-Gly, Phe-Phe-, Leu-Gly, Val-Ala, Phe-Ala, Leu-Phe, Leu-Ala, Phe-Leu-Gly, Phe-Phe-Leu, Leu-Leu-Gly, Phe-Tyr-Ala, Phe-Gly-Phe, Phe-Phe-Gly, Phe-Leu-Gly-Phe, Gly-Phe-Leu-Gly-Phe,Gly-.beta.Ala, Phe-Gly-.beta.Ala, Phe-Phe-.beta.Ala, Leu-Gly-.beta.Ala, Val-Ala-.beta.Ala, Phe-Ala-.beta.Ala, Leu-Phe-.beta.Ala, Leu-Gly-.beta.Ala, Phe-Leu-Gly-.beta.Ala, Phe-Phe-Leu .beta.Ala, Leu-Leu-Gly-.beta.Ala, Phe-Tyr-Ala-.beta.Ala, Phe-Gly-Phe-.Type: GrantFiled: July 27, 1995Date of Patent: October 29, 1996Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Nicola Mongelli, Francesco Angelucci, Enrico Pesenti, Antonino Suarato, Giovanni Biasoli
-
Patent number: 5547667Abstract: Conjugates of general formula 1:[A--O--W--Z].sub.a --T 1wherein the moiety A--O-- is the residue of drug of formula A--O--H in which --O--H is a primary or secondary hydroxyl group; a is an integer of from 1 to 30; W is a group of general formula 2: ##STR1## wherein b is an integer of from 1 to 4, B represents a C.sub.1 -C.sub.3 alkylene group and R.sub.1 and R.sub.2 each independently represent hydrogen, halogen, alkyl, phenyl or substituted phenyl; Z is a spacer group and T is a carrier moiety.Type: GrantFiled: October 25, 1994Date of Patent: August 20, 1996Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Francesco Angelucci, Laura Bersani, Michele Caruso, Marina Ripamonti, Daniela Ruggieri, Antonino Suarato
-
Patent number: 5473055Abstract: A polymer conjugate consisting essentially of: from 90 to 99.9 mol % of units represented by the formula ##STR1## from 0.1 to 5 mol % of units represented by the formula ##STR2## wherein one of R.sub.1 and R.sub.2 is a copolymer residue of the formula ##STR3## and the other one is hydrogen atom; from 0 to 9.9 mol % of units represented by the formula ##STR4## wherein R is a phenyl or t-butoxy group, R.sub.3 is H or an acetyl group, A and A.sub.1 which may be the same or different, represent a chemical single bond, an amino acid residue or peptide spacer selected from .beta.Ala, Gly, Phe-Gly, Phe-Phe-, Leu-Gly, Val-Ala, Phe-Ala, Leu-Phe, Leu-Ala, Phe-Leu-Gly, Phe-Phe-Leu, Leu-Leu-Gly, Phe-Tyr-Ala, Phe-Gly-Phe, Phe-Phe-Gly, Phe-Leu-Gly-Phe, Gly-Phe-Leu-Gly-Phe,Gly-.beta.Ala, Phe-Gly-.beta.Ala, Phe-Phe-.beta.Ala, Leu-Gly-.beta.Ala, Val-Ala-.beta.Ala, Phe-Ala-.beta.Ala, Leu-Phe-.beta.Ala, Leu-Gly-.beta.Ala, Phe-Leu-Gly-.beta.Ala, Phe-Phe-Leu .beta.Ala, Leu-Leu-Gly-.beta.Ala, Phe-Tyr-Ala-.beta.Ala, Phe-Gly-Phe-.Type: GrantFiled: June 22, 1994Date of Patent: December 5, 1995Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Nicola Mongelli, Francesco Angelucci, Enrico Pesenti, Antonino Suarato, Giovanni Biasoli
-
Patent number: 5412081Abstract: Anthracycline glycosides having the general formula 1 and 2: ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen, fluorine, hydroxy or amino; R.sub.2 and R.sub.3 represent hydroxy or one of R.sub.2 and R.sub.3 is a hydrogen atom, a nitro or an amino group and the other of R.sub.2 and R.sub.3 is a HYDROXY group, exhibit activity against LoVo and LoVo/Dx in vitro.Type: GrantFiled: January 6, 1993Date of Patent: May 2, 1995Assignee: Farmitalia Carlo Erba S.R.L.Inventors: Francesco Angelucci, Alberto Bargiotti, Daniela Faiardi, Stefania Stefanelli, Antonino Suarato
-
Patent number: 5387578Abstract: Conjugate of general formula 1:[A--O--W-Z].sub.a -T 1wherein the moity A--O--is the residue of drug of formula A--O--H in which --O--H is a primary or secondary hydroxyl group; a is an integer of from 1 to 30; W is a group of general formula 2: ##STR1## wherein b is an integer of from 1 to 4, B represents a C.sub.1 -C.sub.3 alkylene group and R.sub.1 and R.sub.2 each independently represent hydrogen, halogen, alkyl, phenyl or substituted phenyl; Z is a spacer group and T is a carrier moiety.Type: GrantFiled: April 3, 1992Date of Patent: February 7, 1995Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Francesco Angelucci, Laura Bersani, Michele Caruso, Marina Ripamonti, Daniela Ruggieri, Antonino Suarato