Patents by Inventor Victor G. Matassa
Victor G. Matassa 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: 7459452Abstract: 4,5-Dihydroxypyrimidine-6-carboxamides of formula: are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein R1, R2, R3 and R4 are defined herein. These compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described.Type: GrantFiled: September 7, 2006Date of Patent: December 2, 2008Assignee: Istituto di Ricerche di Biologia Molecolare P. Angeletti S.p.A.Inventors: Maria E. Di Francesco, Cristina Gardelli, Steven Harper, Victor G. Matassa, Ester Murgalia, Emanuela Nizi, Paola Pace, Barbara Pacini, Alessia Petrocchi, Marco Poma, Vincenzo Summa
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Patent number: 7232819Abstract: 4,5-Dihydroxypyrimidine-6-carboxamides of formula (I); are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein R1, R2, R3 and R4 are defined herein. These compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: GrantFiled: October 21, 2002Date of Patent: June 19, 2007Assignee: Istituto Di Ricerche Di Biologia P. Angeletti S.p.A.Inventors: Maria E. Di Francesco, Cristina Gardelli, Steven Harper, Victor G. Matassa, Ester Murgalia, Emanuela Nizi, Paola Pace, Barbara Pacini, Alessia Petrocchi, Marco Poma, Vincenzo Summa
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Patent number: 5618812Abstract: Compounds of Formula (I), and salts and prodrugs thereof, wherein R.sup.1 represents H, optionally substituted C.sub.1-6 alkyl or C.sub.3-7 cycloalkyl; R.sup.2 is NHR.sup.12 or (CH.sub.2).sub.s R.sup.13 where 5 is 0, 1 or 2; R.sup.3 represents C.sub.1-6 alkyl, halo or NR.sup.6 R.sup.7 ; R.sup.4 and R.sup.5 are H, C.sub.1-12 alkyl optionally substituted by NR.sup.9 R.sup.9' or an azacyclic or azabicyclic group, optionally substituted C.sub.4-9 cycloalkyl, C.sub.4-9 cycloalkyl C.sub.1-4 alkyl, aryl, arylC.sub.1-6 alkyl or azacyclic or azabicyclic groups, or R.sup.4 and R.sup.5 together form the residue of an optionally substituted azacyclic or azabicyclic ring system; x is 0, 1, 2 or 3; R.sup.12 is optionally substituted phenyl or pyridyl; R.sup.13 represents a group (A) wherein R.sup.14 is H or C.sub.1-6 alkyl; R.sup.15 is H, C.sub.1-6 alkyl, halo or NR.sup.6 R.sup.7 ; and the dotted line is an optional covalent bond; are CCK and/or gastrin antagonists useful in therapy.Type: GrantFiled: January 26, 1995Date of Patent: April 8, 1997Assignee: Merck Sharp & Dohme, Ltd.Inventors: Jose L. Castro Pineiro, William R. Carling, Mark S. Chambers, Stephen R. Fletcher, Sarah C. Hobbs, Victor G. Matassa, Kevin W. Moore, Graham A. Showell, Michael G. Russell
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Patent number: 5607957Abstract: A class of substituted imidazole, triazole and tetrazole derivatives are selective agonists of 5-HT.sub.1 -like receptors and are therefore useful in the treatment of clinical conditions, in particular migraine and associated disorders, for which a selective agonist of these receptors is indicated.Type: GrantFiled: September 29, 1994Date of Patent: March 4, 1997Assignee: Merck Sharp & Dohme Ltd.Inventors: Jose L. Castro Pineiro, Victor G. Matassa
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Patent number: 5604240Abstract: A class of substituted pyrrolo[2,3-c]pyridine derivatives are selective agonists of 5-HT.sub.1 -like receptors and are therefore useful in the treatment of clinical conditions, in particular migraine and associated disorders, for which a selective agonist of these receptors is indicated.Type: GrantFiled: November 16, 1995Date of Patent: February 18, 1997Assignee: Merck, Sharp & Dohme, Ltd.Inventors: Mark S. Chambers, Victor G. Matassa
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Patent number: 5602163Abstract: A class of substituted imidazole, triazole and tetrazole derivatives are selective agonists of 5-HT.sub.1 -like receptors and are therefore useful in the treatment of clinical conditions, in particular migraine and associated disorders, for which a selective agonist of these receptors is indicated.Type: GrantFiled: May 25, 1995Date of Patent: February 11, 1997Assignee: Merck, Sharp & Dohme Ltd.Inventors: Raymond Baker, Victor G. Matassa, Leslie J. Street
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Patent number: 5602162Abstract: A class of substituted imidazole, triazole and tetrazole derivatives are selective agonists of 5-HT.sub.1 -like receptors and are therefore useful in the treatment of clinical conditions, in particular migraine and associated disorders, for which a selective agonist of these receptors is indicated.Type: GrantFiled: May 10, 1995Date of Patent: February 11, 1997Assignee: Merck, Sharp & Dohme Ltd.Inventors: Raymond Baker, Victor G. Matassa, Leslie J. Street
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Patent number: 5602125Abstract: Thienodiazepine compounds of formula (1) wherein: R.sup.1 represents H, optionally substituted C.sub.1-6 alkyl or C.sub.3-7 cycloalkyl; R.sup.2 represents optionally substituted phenyl; or R.sup.2 represents a group (a) where W is CH.sub.2 or NR.sup.9 and W.sup.1 is CH.sub.2 or W and W.sup.1 are each O; R.sup.3 is C.sub.3-7 cycloalkyl optionally substituted by one or more C.sub.1-4 alkyl groups, or R.sup.3 is NR.sup.11 R.sup.12, where R.sup.11 and R.sup.12 are each H; C.sub.1-12 alkyl optionally substituted by NR.sup.9 R.sup.9 or an azacyclic or azabicyclic group; C.sub.4-9 cycloalkyl optionally substituted by one or more C.sub.1-4 alkyl groups; C.sub.4-9 cycloalkylC.sub.1-4 alkyl optionally substituted in the cycloalkyl ring by one or more C.sub.1-4 alkyl groups; optionally substituted aryl; optionally substituted arylC.sub.1-6 alkyl; or azacyclic or azabicyclic groups; or R.sup.11 and R.sup.Type: GrantFiled: February 28, 1995Date of Patent: February 11, 1997Assignee: Merck, Sharp & Dohme, Ltd.Inventors: William R. Carling, Victor G. Matassa
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Patent number: 5597915Abstract: Compounds of Formula (I), and salts and prodrugs thereof wherein: R.sup.1 is H, certain optionally substituted C.sub.1-6 alkyl or C.sub.3-7 cycloalkyl; R.sup.2 represents a group (a) wherein X is O, S or NR.sup.8 where R.sup.8 is H or C.sub.1-4 alkyl; one of Z and Y is C.dbd.O and the other is O, S or NR.sup.9, where R.sup.9 is H or C.sub.1-4 alkyl; R.sup.3 is C.sub.1-6 alkyl, halo or NR.sup.6 R.sup.7 ; R.sup.4 is C.sub.3-10 cycloalkyl; n is 0, 1, 2 or 3, and are CCK and/or gastrin antagonists, which compounds and compositions thereof are useful in therapy.Type: GrantFiled: September 15, 1994Date of Patent: January 28, 1997Assignee: Merck Sharp & Dohme Ltd.Inventors: Mark S. Chambers, Stephen R. Fletcher, Victor G. Matassa, Mark G. Bock
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Patent number: 5583152Abstract: The invention concerns novel, pharmaceutically useful, amide derivatives of certain benzoheterocyclylalkanoic acids (and related tetrazoles and acylsulphonamides) of the formula I and salts thereof, wherein the radicals R.sup.1, R.sup.2, L, X, Y, Z, A.sup.1, Q, A.sup.2 and M have the meanings set out in the specification. The invention also includes pharmaceutical compositions incorporating a formula I compound or a salt thereof, a process for the manufacture of the said compound, together with intermediates for use in the latter process.Type: GrantFiled: June 5, 1995Date of Patent: December 10, 1996Assignee: Zeneca Inc.Inventors: Peter R. Bernstein, Frederick J. Brown, Victor G. Matassa, Ying K. Yee
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Patent number: 5567726Abstract: Imidazole, triazole and tetrazole derivatives of formula (I) are selective agonists of 5-HT.sub.1 -like receptors and are therefore useful in the treatment of clinical conditions, in particular migraine and associated disorders, for which a selective agonist of these receptors is indicated, wherein the broken circle represents two non-adjacent double bonds in any position in the five-membered ring; two, three or four of V, W, X, Y and Z represent nitrogen and the remainder represent carbon provided that, when two of V, W, X, Y and Z represent nitrogen and the remainder represent carbon, then the said nitrogen atoms are in non-adjacent positions within the five-membered ring; E represents a bond or a straight or branched alkylene chain containing from 1 to 4 carbon atoms; F represents a group of formula (a); U represents nitrogen or C--R.sup.2 ; B represents oxygen, sulphur or N--R.sup.3 ; R.sup.1 represents a group of formula (i), (ii) or (iii).Type: GrantFiled: January 24, 1995Date of Patent: October 22, 1996Assignee: Merck, Sharp & Dohme Ltd.Inventors: Raymond Baker, Jose L. Castro Pineiro, Alexander R. Guiblin, Austin J. Reeve, Francine Sternfeld, Victor G. Matassa, Leslie J. Street
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Patent number: 5554629Abstract: A discrete class of 4-substituted 1,2,4-triazole derivatives are selective agonists of 5-HT.sub.1 -like receptors and are therefore useful in the treatment of clinical conditions, in particular migraine and associated disorders, for which a selective agonist of these receptors is indicated.Type: GrantFiled: June 29, 1995Date of Patent: September 10, 1996Assignee: Merck, Sharp & Dohme Ltd.Inventors: Raymond Baker, Victor G. Matassa, Austin J. Reeve, Francine Sternfeld, Leslie J. Street
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Patent number: 5527817Abstract: The sulphate salt of N,N-dimethyl-2-[5-(1,2,4-triazol-1-ylmethyl)-1H-indol-3-yl]ethylamine is a selective agonist of 5-HT.sub.1 -like receptors and is therefore useful in the treatment of clinical conditions, in particular migraine and associated disorders, for which a selective agonist of these receptors is indicated.Type: GrantFiled: December 7, 1994Date of Patent: June 18, 1996Assignee: Merck Sharp & Dohme LimitedInventors: Raymond Baker, Victor G. Matassa, Alexander R. Guiblin, Kendal G. Pitt, Leslie J. Street, Carole Olive, David E. Storey
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Patent number: 5521175Abstract: Compounds of Formula (I), and salts and prodrugs thereof, wherein R.sup.1 represents C.sub.1-6 alkyl or C.sub.3-7 cycloalkyl; R.sup.2 optionally substituted phenyl or R.sup.2 represents a group (A) where W is CH.sub.2 or NR.sup.10, and W.sup.1 is CH.sub.2, or W and W.sup.1 each represent 0; R.sup.3 is C.sub.1-6 alkyl, halo or NR.sup.13 R.sup.14 ; R.sup.4 is H, C.sub.1-4 alkyl, optionally substituted phenyl or optionally substituted benzyl; R.sup.5, R.sup.6, R.sup.7 and R.sup.8 are H or C.sub.1-4 alkyl; or any two of R.sup.4, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 together form a chain (CH.sub.2).sub.t, and any other two of R.sup.4, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 optionally form a chain (CH.sub.2).sub.s where s and t are independently 1, 2 or 3; m is 2, 3, 4, 5, 6, 7, 8 or 9; n is 0, 1, 2, 3 or 4; and x is 0, 1, 2 or 3; are CCK and/or gastrin antagonists useful in therapy.Type: GrantFiled: January 26, 1995Date of Patent: May 28, 1996Assignee: Merck Sharp & Dohme Ltd.Inventors: Jose L. Castro Pineiro, Mark S. Chambers, Victor G. Matassa
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Patent number: 5510362Abstract: A class of substituted imidazole, triazole and tetrazole derivatives of formula (I), wherein the broken circle represents two non-adjacent double bonds in any position in the five-membered ring; two, three or four of V,W,X,Y and Z represent nitrogen and the remainder represent carbon provided that, when two of V,W,X,Y and Z represent nitrogen and the remainder represent carbon, then the said nitrogen atoms are in non-adjacent positions within the five-membered ring; E represents a bond or a straight or branched alkylene chain containing from 1 to 4 carbon atoms; F represents a group of formula (lI); U represents nitrogen or C--R.sup.2 ; B represents oxygen, sulphur or N--R.sup.3 ; are selective agonists of 5--HT.sub.1 -like receptors and are therefore useful in the treatment of clinical conditions, in particular migraine and associated disorders, for which a selective agonist of these receptors is indicated.Type: GrantFiled: September 8, 1994Date of Patent: April 23, 1996Assignee: Merck, Sharp and Dohme LimitedInventors: Victor G. Matassa, Austin J. Reeve, Francine Sternfeld, Helen Routledge, Leslie Street
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Patent number: 5510359Abstract: A class of substituted five-membered heteroaromatic compounds possessing an imino spacer group are selective agonists of 5-HT.sub.1 -like receptors and are therefore useful in the treatment of clinical conditions, in particular migraine and associated disorders, for which a selective agonist of these receptors is indicated.Type: GrantFiled: October 7, 1994Date of Patent: April 23, 1996Assignee: Merck Sharp & Dohme Ltd.Inventors: Jose L. Castro Pineiro, Victor G. Matassa
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Patent number: 5451582Abstract: Compounds of formula (I), and salts and prodrugs thereof ##STR1## wherein: R.sup.1 is H, certain optionally substituted C.sub.1.6 alkyl, or C.sub.3-7 cycloalkyl;R.sup.2 is (CH.sub.2).sub.q -tetrazolyl optionally substituted in the tetrazole ring by C.sub.1-4 alkyl, (CH.sub.2).sub.q -imidazolyl (where q is 0, 1, 2 or 3), CONHSO.sub.2 R.sup.9, SO.sub.2 NHCOR.sup.9 (where R.sup.9 is C.sub.1-6 alkyl, optionally substituted aryl or trifluoromethyl). SO.sub.2 NHR.sup.10 (where R.sup.10 is a nitrogen containing heterocycle), cyclopropyl or (CH.sub.2), CO.sub.2 H, where n is 1 or 2;R.sup.3 is C.sub.1-6 alkyl, halo or NR.sup.6 R.sup.7 ;R.sup.4 is C.sub.1-7 straight or branched chain alkyl; andx is 0, 1, 2 or 3;are CCK and/or gastrin receptor antagonists. They and compositions thereof are useful in therapy.Type: GrantFiled: February 12, 1993Date of Patent: September 19, 1995Assignee: Merck Sharp & Dohme Ltd.Inventors: Mark S. Chambers, Victor G. Matassa, Stephen R. Fletcher
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Patent number: 5451588Abstract: A class of substituted imidazole, triazole and tetrazole derivatives are selective agonists of 5-HT.sub.1 -like receptors and are therefore useful in the treatment of clinical conditions, in particular migraine and associated disorders, for which a selective agonist of these receptors is indicated.Type: GrantFiled: November 22, 1993Date of Patent: September 19, 1995Assignee: Merck Sharp & Dohme Ltd.Inventors: Raymond Baker, Victor G. Matassa, Leslie J. Street
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Patent number: 5440035Abstract: The invention concerns novel, pharmaceutically useful, amide derivatives of certain benzoheterocyclylalkanoic acids (and related tetrazoles and acylsulphonamides) of the formula I and salts thereof, wherein the radicals R.sup.1, R.sup.2, L, X, Y, Z, A.sup.1, Q, A.sup.2 and M have the meanings set out in the specification. The invention also includes pharmaceutical compositions incorporating a formula I compound or a salt thereof, a process for the manufacture of the said compound, together with intermediates for use in the latter process.Type: GrantFiled: October 25, 1994Date of Patent: August 8, 1995Assignee: Zeneca Inc.Inventors: Peter R. Bernstein, Frederick J. Brown, Victor G. Matassa, Ying K. Yee
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Patent number: 5391758Abstract: The invention concerns novel, pharmaceutically useful, amide derivatives of certain benzoheterocyclylalkanoic acids (and related tetrazoles and acylsulphonamides) of the formula I and salts thereof, wherein the radicals R.sup.1, R.sup.2, L, X, Y, Z, A.sup.1, Q, A.sup.2 and M have the meanings set out in the specification. The invention also includes pharmaceutical compositions incorporating a formula I compound or a salt thereof, a process for the manufacture of the said compound, together with intermediates for use in the latter process.Type: GrantFiled: June 6, 1994Date of Patent: February 21, 1995Assignee: Zeneca, Inc.Inventors: Peter R. Bernstein, Frederick J. Brown, Victor G. Matassa, Ying K. Yee