Patents by Inventor Angelo Bedeschi
Angelo Bedeschi 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).
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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
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Patent number: 5621096Abstract: The invention provides a process for the preparation of the compound of formula I ##STR1## wherein R is carboxy group or a carboxylate anion, by enzymatic hydrolysis with a lipase or an acylase in an alcoholic solution, of a compound of the formula II ##STR2## wherein R.sub.1, represents a hydrogen atom or a C.sub.1 -C.sub.6 alkyl group, and R.sub.2 is a hydrogen atom, an alkyl, alkenyl, phcnyl, phenylalkyl or phenylalkenyl group having from 1 to 18 carbon atoms or an alkoxy group.Type: GrantFiled: November 16, 1995Date of Patent: April 15, 1997Assignee: Pharmacia S.p.A.Inventors: Walter Cabri, Angelo Bedeschi
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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
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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
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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
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Patent number: 5457193Abstract: The present invention relates the removal of t-butyldimethylsilyl protecting groups in the preparation of penems which are useful antibiotics. The invention provides a process for preparing a compound of the formula I: ##STR1## wherein R is a free or protected hydroxy or amino group or an alkoxy, acyloxy or an optionally substituted carbamoyloxy group, and R.sub.1 is selected from:a) hydrogen;b) a C.sub.2 -C.sub.4 alkenyl group;c) a p-NO.sub.2 benzyl group;d) a linear or branched alkanoyloxy C.sub.1 -C.sub.2 alkyl group; ande) (2-oxo-1,3-dioxolen-4-yl)methyl optionally substituted by C.sub.1 -C.sub.Type: GrantFiled: March 6, 1995Date of Patent: October 10, 1995Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Angelo Bedeschi, Franco Zarini
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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
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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
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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
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Patent number: 5360904Abstract: A process for preparing penem esters by reacting ##STR1## wherein R.sub.1 is a hydroxy protecting group and X is a C.sub.1 -C.sub.10 alkyl or aryl group, with ##STR2## wherein R.sub.2 is hydrogen or a C.sub.1 -C.sub.6 alkyl group in the presence of an anhydrous organic solvent, condensing the product with ##STR3## wherein X is a halogen atom or a --OCOOR.sub.3 group and then cyclizing.Type: GrantFiled: September 21, 1992Date of Patent: November 1, 1994Assignee: Farmitalia Carlo Erba S r lInventors: Angelo Bedeschi, Walter Cabri, Marcello Marchi, Ettore Perrone
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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
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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
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Patent number: 4886793Abstract: There are provided compounds of formula I: ##STR1## wherein R.sup.1 is hydrogen or a C.sub.1 -C.sub.4 alkyl group either unsubstituted or substituted by one or more substituents chosen from a free or protected hydroxy or halogen atom;R.sup.2 is a free or esterified carboxy group or carboxylate anion;R.sup.3 and R.sup.4 are each independently hydrogen or organic group,X is --O--, ##STR2## --S--, Q is either(a") free or protected hydroxy, or(b") a C.sub.1 -C.sub.1 acyloxy, or(c") carbamoyloxy OCONH.sub.2, or(d") an optionally substituted heterocyclylthio group, or(e") an optionally substituted imido group, or(f") an optionally substituted quaternary ammonium group or(g") a halogen atom,A and the pharmaceutically or veterinarily acceptable salts thereof. There are provided also methods for preparing compounds of formula I. The compounds of formula I are useful as antibacterial agents.Type: GrantFiled: March 5, 1987Date of Patent: December 12, 1989Assignee: Farmitalia Carlo Erba, S.r.l.Inventors: Ettore Perrone, Marco Alpegiani, Angelo Bedeschi, Franco Zarini, Costantino Della Bruna, Giovanni Franceschi
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Patent number: 4863914Abstract: Compounds of formula ##STR1## wherein R is hydrogen atom or C.sub.1 -C.sub.4 alkyl group optionally substituted from halogen atom or hydroxy group optionally protected, A is a Z, Z--O--C--O-- or Z--C)-- residue, wherein Z is phenylene, naphthylene, heterocyclediyl, C.sub.1 -C.sub.7 alkylene, C.sub.2 -C.sub.4 alkenylene, alkynylene, ##STR2## C.sub.3 -C.sub.8 cycloalkylene, aralkylene radical optionally substituted, and O.sup.(+) represents a group +NR.sub.1 R.sub.2 R.sub.3, wherein R.sub.1, R.sub.2 and R.sub.3 are each either:(i) a optionally substituted alkyl, aralkyl or aryl radical or(ii) R.sub.1 is as defined above under (i) and R.sub.2 and R.sub.3, taken together, represent an optionally substituted or fused heterocyclic radical, or(iii) R.sub.1, R.sub.2 and R.sub.3, taken together, represent an optionally substituted azonia-bicyclo or tricyclo radical, or(iv) R.sub.1, R.sub.2 and R.sub.Type: GrantFiled: April 8, 1986Date of Patent: September 5, 1989Assignee: Farmitalia Carlo ErbaInventors: Ettore Perrone, Marco Alpegiani, Angelo Bedeschi, Franco Zarini, Giovanni Franceschi, Costantino D. Bruna
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Patent number: 4837215Abstract: Compounds of the following formula I ##STR1## wherein X represents a sulphur or an oxygen atom,R is hydrogen or a C.sub.1 -C.sub.4 alkyl group either unsubstituted or substituted by one or more substituents chosen from a free or protected hydroxy group and halogen atom;A is a Z, Z--O--CO-- or --Z--CO-- residue, whereinZ represents(a) an optionally substituted phenylene or naphthylene group,(b) an optionally substituted heterocyclediyl radical wherein the hetero ring is mono or bicyclic, saturated or unsaturated containing at least one heteroatom selected from the group of oxygen, sulphur and nitrogen;(c) an optionally substituted linear or branched C.sub.1 -C.sub.7 alkylene radical;(d) a C.sub.2 -C.sub.4 alkenylene or alkynylene group or a group of formula ##STR2## (e) an optionally substituted C.sub.3 -C.sub.8 cycloalkylene ring; (f) an aralkylene radical of the formula ##STR3## wherein n is 1, 2 or 3; andQ.sup.(+) represents a +NR.sub.1 R.sub.2 R.sub.3 group, wherein(i) R.sub.1, R.sub.2, R.sub.Type: GrantFiled: April 8, 1986Date of Patent: June 6, 1989Assignee: Farmitalia Carlo ErbaInventors: Ettore Perrone, Marco Alpegiani, Angelo Bedeschi, Franco Zarini, Giovanni Franceschi, Costantino D. Bruna
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Patent number: 4771134Abstract: Compounds of formula I ##STR1## wherein R.sub.1 and R.sub.2 is each H, halo or an organic group, R.sub.3 is H or organic group, n=1 or 2, M is a heavy mono- or divalent metal, or M.sub.2 A wherein M.sub.2 is a heavy divalent metal and A is an organic or inorganic group, are prepared by treating a starting penicillin in a solvent with a salt of M.sub.1 or M.sub.2 A in the presence of a base at a temperature of from -70.degree. to 100.degree. C.Type: GrantFiled: January 13, 1986Date of Patent: September 13, 1988Assignee: Farmitalia Carlo Erba S.p.A.Inventors: Marco Alpegiani, Angelo Bedeschi, Ettore Perrone
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Patent number: 4760058Abstract: Described is a novel process for the preparation of penams and penems useful as antibacterial agents, which comprises the reaction of an appropriate f-substituted-azetidin-2-one with a base, followed by reaction of the thereby formed penam compound with an oxidating agent and an organic or inorganic base.Also described are novel pemam compounds useful as antibacterials which are prepared by the described process.Type: GrantFiled: December 10, 1986Date of Patent: July 26, 1988Assignee: Farmitalia Carlo Erba S.p.A.Inventors: Stephen Hanessian, Angelo Bedeschi
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Patent number: 4729990Abstract: Antibacterial compounds of formula (I) ##STR1## wherein, R.sub.1 ' is alkyl or hydroxyalkyl;R.sub.2 is hydrogen or a carboxy protecting group; andY' is a group-S-heterocyclic or pyridyl, which group may be substituted, and pharmaceutically or veterinarily acceptable salts thereof and pharmaceutical compositions containing the same.Type: GrantFiled: December 11, 1985Date of Patent: March 8, 1988Assignee: Farmitalia Carlo Erba S.p.A.Inventors: Marco Alpegiani, Angelo Bedeschi, Maurizio Foglio, Giovanni Francheschi, Ettore Perrone
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Patent number: 4713450Abstract: A new process is described for the preparation of (5R)-penem derivatives of the general formula I: ##STR1## wherein R.sub.1 represents a hydrogen atom or an organic group; R.sub.2 represents a hydrogen atom or a carboxy protecting group and Y represents a hydrogen or halogen atom or an organic group. A 2-thiacephem derivative of the general formula II: ##STR2## wherein R.sub.1, R.sub.2 and Y have the meanings/given above is oxidized by means of organic peracids to the corresponding sulphone of the general formula III: ##STR3## which is subsequently submitted to a desulphurative ring contraction by extrusion of SO.sub.2 to give exclusively the desired (5R)-penem derivatives of the general formula I.Type: GrantFiled: January 24, 1986Date of Patent: December 15, 1987Assignee: Farmitalia Carlo Erba S.p.A.Inventors: Marco Alpegiani, Angelo Bedeschi, Maurizio Foglio, Giovanni Franceschi, Ettore Perrone
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Patent number: 4663451Abstract: Described is a novel process for the preparation of penams and penems useful as antibacterial agents, which comprises the reaction of an appropriate 4-substituted-azetidin-2-one with a base, followed by reaction of the thereby formed penam compound with an oxidating agent and a organic or inorganic base.Also described are novel penam compounds useful as antibacterials which are prepared by the described process.Type: GrantFiled: August 29, 1984Date of Patent: May 5, 1987Assignee: Farmitalia Carlo Erba S.p.A.Inventors: Stephen Hanessian, Angelo Bedeschi