The Nitrogen Is Bonded Directly At 4- Or 6-position Patents (Class 544/317)
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Patent number: 7371860Abstract: This application relates to monomers of the general formula (I) for the preparation of PNA (peptide nucleic acid) oligomers and provides method for the synthesis of both predefined sequence PNA oligomers and random sequence PNA oligomers: wherein E is nitrogen or C—R?; J is sulfur or oxygen; R?, R1, R2, R3, R4 is independently H, halogen, alkyl, nitro, nitrite, alkoxy, halogenated alkyl, halogenated alkoxy, phenyl or halogenated phenyl, R5 is H or protected or unprotected side chain of natural or unnatural ?-amino acid; and B is a natural or unnatural nucleobase, wherein when said nucleobase has an exocyclic amino function, said function is protected by protecting group which is labile to acids but stable to weak to medium bases in the presence of thiol.Type: GrantFiled: July 15, 2005Date of Patent: May 13, 2008Assignee: Panagene, Inc.Inventors: Sung Kee Kim, Hyunil Lee, Jong Chan Lim, Hoon Choi, Jae Hoon Jeon, Sang Youl Ahn, Sung Hee Lee, Won Jun Yoon
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Publication number: 20080015185Abstract: N-heterocyclic compounds that block cytokine production via inhibition of p38 kinase are disclosed. In one embodiment, compounds of the present invention are represented by Formula (I): Methods of production, pharmaceutical compositions and methods of treating conditions associated with inappropriate p38 kinase activity or TNF-? expression utilizing compounds of the present invention are also disclosed.Type: ApplicationFiled: July 16, 2007Publication date: January 17, 2008Inventors: Gulzar Ahmed, Axel Metzger, Ian Henderson, David J. Diller, Jun Wen, Stephen T. Wrobleski, Katerina Leftheris, Chunjian Liu
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Patent number: 7314934Abstract: Novel substituted 2,4,8-trisubstituted-8H-pyrido[2,3-d]pyrimidin-7-one compounds and compositions for use in therapy as CSBP/p38 kinase inhibitors.Type: GrantFiled: August 19, 2003Date of Patent: January 1, 2008Assignee: SmithKline Beecham CorporationInventors: Jerry L. Adams, Jeffrey C. Boehm, Ralph Hall, Qi Jin, Jiri Kasparec, Domingos J. Silva, John J. Taggart
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Patent number: 7312180Abstract: A description is given of 4-(4-trifluoromethylpyrazolyl)pyrimidines of the formula (I) and of their use as herbicides. In this general formula (I), R1, R2, R3 and R4 are various radicals and Y is an aromatic or heteroaromatic radical.Type: GrantFiled: March 10, 2005Date of Patent: December 25, 2007Assignee: Bayer CropScience GmbHInventors: Michael Gerhard Hoffmann, Hendrik Helmke, Lothar Willms, Thomas Auler, Heinz Kehne, Martin Hills, Dieter Feucht
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Patent number: 7294627Abstract: Compounds of formula (I) in which R1, R2, R3 and R4, have the meanings given in the specification are Factor Xa inhibitors useful in the treatment of thrombotic disorders.Type: GrantFiled: December 9, 2002Date of Patent: November 13, 2007Assignee: Eli Lilly and CompanyInventors: Steven Douglas Hiscock, Stuart Donald Jones, Daniel Jon Sall, Stephen Clinton Young, Michael Robert Wiley
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Patent number: 7285533Abstract: A novel cytokine, designated Apo-2 ligand, which induces mammalian cell apoptosis is provided. The Apo-2 ligand is believed to be a member of the TNF cytokine family. Compositions including Apo-2 ligand chimeras, nucleic acid encoding Apo-2 ligand, and antibodies to Apo-2 ligand are also provided. Methods of using Apo-2 ligand to induce apoptosis and to treat pathological conditions such as cancer, are further provided.Type: GrantFiled: June 4, 2004Date of Patent: October 23, 2007Assignee: Genentech, Inc.Inventor: Avi J. Ashkenazi
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Patent number: 7247633Abstract: A compound of the general formula (I): wherein R1, R2, X, Y and Z are as described in the specification.Type: GrantFiled: July 14, 2003Date of Patent: July 24, 2007Assignee: Biovitrum ABInventor: Björn M. Nilsson
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Patent number: 7235571Abstract: What is described are compounds of the formulae (I) and (II) where the symbols and indices have the meanings given in the description. These compounds are suitable for controlling animal pests.Type: GrantFiled: March 29, 2004Date of Patent: June 26, 2007Assignee: Merial LimitedInventors: Marion Beckmann, Oswald Ort, Uwe Döller, Gerhard Krautstrunk, Wolfgang Schaper, Peter Lümmen, Daniela Jans, Waltraud Hempel, Jutta Maria Waibel, Barbara Lörkens
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Patent number: 7230104Abstract: Pyrimidines of formula I in which R1 represents hydrogen or alkyl, haloalkyl, alkenyl, alkynyl, alkadienyl, alkoxy, cycloalkyl, phenyl, or 5- or 6-membered heteroaryl or 5- or 6-membered heterocyclyl, containing one to four nitrogen atoms or one to three nitrogen atoms and one sulfur or oxygen atom, or tri-alkyl-silyl, formyl or alkoxy-carbonyl, wherein R1 groups are unsubstituted or substituted as defined in the specification; R2 represents phenyl, cycloalkyl or 5- or 6-membered heteroaryl, containing one to four nitrogen atoms or one to three nitrogen atoms and one sulfur or oxygen atom, which are unsubstituted or substituted; R3 represents hydrogen, halogen or alkyl, alkoxy, alkylthio, alkylamino or dialkylamino; which are unsubstituted or substituted; R4 represents hydrogen or alkyl, alkenyl or alkynyl; which are unsubstituted or substituted; and X represents O, S, NR5 or a single bond, wherein R5 represents hydrogen or alkyl; or R1 and R5 together with the interjacent nitrogen atom form a heteroType: GrantFiled: July 22, 2005Date of Patent: June 12, 2007Assignee: BASF AktiengesellschaftInventors: Klaus-Juergen Pees, Waldemar Pfrengle, Gavin Heffernan
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Patent number: 7230100Abstract: A process for producing predominantly cis nucleosides or nucleoside analogues and derivatives of formula (A): wherein R1 is a pyrimidine base or a pharmaceutically acceptable derivative thereof and Q is oxygen, carbon or sulphur, comprising a coupling step of the pyrimidine base with a molecule of formula (B) described herein in a suitable coupling solvent, in the presence of catalytic amounts of an element or combination of elements of groups IB or IIB of the periodic table, a tertiary amine and a Lewis acid to obtained an intermediate of formula (D) which is deprotected in the subsequent step to generate the product of formula (A).Type: GrantFiled: April 7, 2006Date of Patent: June 12, 2007Assignee: Shire BioChem., Inc.Inventor: Qing Yu
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Patent number: 7220736Abstract: A cyclic compound of the formula (I) or a pharmacologically acceptable salt thereof, wherein X is ?CH— or ?N—, Y is —NH—, —NR4—, —S—, —O—, —CH?N—, —N?CH—, —N?N—, —CH?CH—, etc., R1 is a lower alkoxy group, an amino group, a heterocyclic ring containing N atom(s), or a hydroxy group substituted by a heterocyclic ring containing N atom(s) (each of which is optionally substituted), R2 is a lower alkylamino group which is optionally substituted by an aryl group, a lower alkoxy group which is optionally substituted by an aryl group, a lower alkoxy group substituted by an aromatic heterocyclic ring containing N atom(s), R3 is an aryl group, a heterocyclic ring containing N atom(s), a lower alkyl group, a lower alkoxy group, a cyclo lower alkoxy group, a hydroxy group substituted by a heterocyclic ring containing N atom(s), or an amino group (each of which is optionally substituted), and R3 and a substituent in Y may be combined to form a lactone ring.Type: GrantFiled: March 15, 2001Date of Patent: May 22, 2007Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Koichiro Yamada, Kenji Matsuki, Kenji Omori, Kohei Kikkawa
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Patent number: 7211668Abstract: This application relates to monomers of the general formula (I) for the preparation of PNA (peptide nucleic acid) oligomers and provides method for the synthesis of both predefined sequence PNA oligomers and random sequence PNA oligomers: wherein E is sulfur or oxygen; J is nitrogen or C—R?; R1, R? is independently H, halogen, alkyl, nitro, nitrile, alkoxy, halogenated alkyl, halogenated alkoxy or a functional group having one of following general formulae: wherein A1, A2, A3, A4, A5, is independently selected from H, halogen such as F, Cl, Br or I, CF3, alkyl, preferably C1–C4 alkyl, nitro, nitrile, alkoxy, preferably C1–C4 alkoxy, halogenated (such as F, Cl, Br and I) alkyl, preferably halogenated C1–C4 alkyl, halogenated (such as F, Cl, Br and I) alkoxy, preferably halogenated C1–C4 alkoxy, phenyl, and halogenated (such as F, Cl, Br and I phenyl; R2 is H or protected or unprotected side chain of natural or unnatural ?-amino acid; and B is a natural or unnatural nucleobase, wherein when said nucType: GrantFiled: April 6, 2004Date of Patent: May 1, 2007Assignee: Panagene, Inc.Inventors: Sung Kee Kim, Hyunil Lee, Jong Chan Lim, Sung Hee Lee
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Patent number: 7179896Abstract: This application relates to monomers of the general formula (I) for the preparation of PNA (peptide nucleic acid) oligomers and provides method for the synthesis of both predefined sequence PNA oligomers and random sequence PNA oligomers: wherein E is nitrogen or C—R?; J is sulfur or oxygen; R?, R1, R2, R3, R4 is independently H, halogen, alkyl, nitro, nitrile, alkoxy, halogenated alkyl, halogenated alkoxy, phenyl or halogenated phenyl, R5 is H or protected or unprotected side chain of natural or unnatural ?-amino acid; and B is a natural or unnatural nucleobase, wherein when said nucleobase has an exocyclic amino function, said function is protected by protecting group which is labile to acids but stable to weak to medium bases in the presence of thiol.Type: GrantFiled: July 15, 2005Date of Patent: February 20, 2007Assignee: Panagene, Inc.Inventors: Sung Kee Kim, Hyunil Lee, Jong Chan Lim, Hoon Choi, Jae Hoon Jeon, Sang Youl Ahn, Sung Hee Lee, Won Jun Yoon
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Patent number: 7151092Abstract: Compounds of Formula I, their preparation and uses are described: wherein: M and V are cis to one another and MH is cytarabine; the 5? oxygen of said cytarabine is attached to the phosphorus; V is 4-pyridyl; and pharmaceutically acceptable prodrugs and salts thereof.Type: GrantFiled: October 31, 2003Date of Patent: December 19, 2006Assignee: Metabasis Therapeutics, Inc.Inventors: Serge Boyer, Mark D. Erion
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Patent number: 7138404Abstract: This invention is 4-aminopyrimidine derivatives of the formula wherein R1, R2, R3 and R4 are as defined in the specification or a pharmaceutically acceptable salt thereof. The invention also is the preparation of compounds of formula I, pharmaceutical compositions containing therapeutically effective amounts of compounds of formula I or pharmaceutically acceptable salts thereof and to a method of treatment comprising administering therapeutically effective amounts of the compound of formula I for the prevention or treatment of mGluR5 receptor mediated disorders.Type: GrantFiled: April 29, 2002Date of Patent: November 21, 2006Assignee: Hoffmann-La Roche Inc.Inventors: Vincent Mutel, Jens-Uwe Peters, Juergen Wichmann
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Patent number: 7129239Abstract: Compounds of Formula (I) that act as cannabinoid receptor ligands and their uses in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals are described herein. wherein A is an optionally substituted aryl or an optionally substituted heteroaryl; B is an optionally substituted aryl or an optionally substituted heteroaryl; R1 is hydrogen, (C1–C4)alkyl, halo-substituted (C1–C4)alkyl, or (C1–C4)alkoxy; and R4 is as described herein.Type: GrantFiled: October 20, 2003Date of Patent: October 31, 2006Assignee: Pfizer Inc.Inventor: David A. Griffith
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Patent number: 7122552Abstract: The present invention provides a compound of formula I: or a pharmaceutically acceptable salt thereof. These compounds are inhibitors of protein kinases, particularly inhibitors of JAK and CDK2 mammalian protein kinases. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of utilizing those compounds and compositions in the treatment of various protein kinase mediated disorders.Type: GrantFiled: May 30, 2003Date of Patent: October 17, 2006Assignee: Vertex Pharmaceuticals IncorporatedInventor: Brian E. Ledford
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Patent number: 7119202Abstract: Disclosed are compounds of the formula wherein R1 is hydrogen or an acyl group having 1 to 16 carbon atoms; R2 is a purine or pyrimidine base or an analogue or derivative thereof; Z is O, S, S?O or SO2; and pharmaceutically acceptable derivatives thereof. Also described are processes for and intermediates of use in their preparation, pharmaceutical compositions containing these compounds, and the use of these compounds in the antiviral treatment of mammals.Type: GrantFiled: June 6, 1995Date of Patent: October 10, 2006Assignee: Glaxo Wellcome Inc.Inventors: Pierrette Belleau, legal representative, Paul Nguyen Ba, Bernard Belleau, deceased
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Patent number: 7115740Abstract: Disclosed are novel pyrimido compounds that are selective inhibitors of both KDR and FGFR kinases. These compounds and their pharmaceutically acceptable salts are anti-proliferative agents useful in the treatment or control of solid tumors, in particular breast, colon, lung and prostate tumors. Also disclosed are pharmaceutical compositions containing these compounds and methods of treating cancer.Type: GrantFiled: April 2, 2004Date of Patent: October 3, 2006Assignee: Hoffmann-la Roche Inc.Inventors: Yi Chen, Apostolos Dermatakis, Jin-Jun Liu, Kin-Chun Luk, Christophe Michoud, Pamela Loreen Rossman
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Patent number: 7109334Abstract: A process for producing predominantly cis nucleosides or nucleoside analogues and derivatives of formula (A): wherein R1 is a pyrimidine base or a pharmaceutically acceptable derivative thereof and Q is oxygen, carbon or sulphur, comprising a coupling step of the pyrimidine base with a molecule of formula (B) described herein in a suitable coupling solvent, in the presence of catalytic amounts of an element or combination of elements of groups IB or IIB of the periodic table, a tertiary amine and a Lewis acid to obtained an intermediate of formula (D) which is deprotected in the subsequent step to generate the product of formula (A).Type: GrantFiled: June 14, 2002Date of Patent: September 19, 2006Assignee: Shire BioChem, Inc.Inventor: Qing Yu
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Patent number: 7105666Abstract: The present invention provides a method for producing 2-, 6-, 8- and 9-substituted purine compounds from 4,6-dihalo-5-nitro-2-alkyl-pyrimidine compounds in solution or by solid phase techniques. The present process provides for the sequential introduction of amine substituents at the 4- and 6-positions, displacement of an alkylsulfony group at the 2-position of the pyrimidine, reduction of the nitro group and formation of the imidazole portion of the purine compound. Furthermore, the methods of the present invention are ideally suited to the preparation of a library of purine compounds.Type: GrantFiled: June 27, 2003Date of Patent: September 12, 2006Assignee: Roche Palo Alto LLCInventors: Lars G.J. Hammarström, Nancy Elisabth Krauss, Sharada Shenvi Labadie, David Bernard Smith, Francisco Xavier Talamas
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Patent number: 7098197Abstract: The present invention relates to phosphonate compounds, compositions containing them, processes for obtaining them, and their use for treating a variety of medical disorders, e.g., osteoporosis and other disorders of bone metabolism, cancer, viral infections, and the like.Type: GrantFiled: April 6, 2005Date of Patent: August 29, 2006Assignee: The Regents of the University of CaliforniaInventors: Karl Y. Hostetler, James R. Beadle, Ganesh D. Kini
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Patent number: 7094772Abstract: The present invention relates to phosphonate compounds, compositions containing them, processes for obtaining them, and their use for treating a variety of medical disorders, e.g., osteoporosis and other disorders of bone metabolism, cancer, viral infections, and the like.Type: GrantFiled: April 6, 2005Date of Patent: August 22, 2006Assignee: The Regents of the University of CaliforniaInventors: Karl Y. Hostetler, James R. Beadle, Ganesh D. Kini
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Patent number: 7091343Abstract: The present invention relates to compounds useful of inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.Type: GrantFiled: March 14, 2003Date of Patent: August 15, 2006Assignee: Vertex Pharmaceuticals IncorporatedInventors: David Bebbington, Hayley Binch, Jean-Damien Charrier, Simon Everitt, Julian M. C. Golec, David Kay, Ronald Knegtel, Andrew Miller, Francoise Pierard
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Patent number: 7087616Abstract: This invention relates to novel pyrazolylpyrimidines of the formula in which R1, R2, X, n, Y, Z and R have the meanings given in the disclosure, to a plurality of processes for preparing these substances, and to their use for controlling pests.Type: GrantFiled: February 11, 2002Date of Patent: August 8, 2006Assignee: Bayer CropScience AGInventors: Rüdiger Fischer, Bernd Alig, Thomas Bretschneider, Mazen Es-Sayed, Christoph Erdelen, Peter Lösel, Udo Reckmann
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Patent number: 7067664Abstract: Corticotropin-releasing factor (CRF) antagonists having the formulae wherein the dashed lines, A, B, Y, Z, G, R3, R4, R5, R6, R16 and R17 are as defined in the application, and processes for preparing them. These compounds and their pharmaceutically acceptable salts are useful in the treatment disorders including CNS and stress-related disorders.Type: GrantFiled: May 30, 2000Date of Patent: June 27, 2006Assignees: Pfizer Inc., Pfizer Products Inc.Inventor: Yuhpyng L. Chen
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Patent number: 7053213Abstract: Pharmaceutical compositions containing novel therapeutic heterocycles for use in diseases in which an NK2 receptor is implicated, processes for preparing and methods for using the same.Type: GrantFiled: August 30, 2002Date of Patent: May 30, 2006Assignee: AstraZeneca ABInventor: Scott Carson Miller
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Patent number: 7034014Abstract: The present invention relates to phosphonate compounds, compositions containing them, processes for obtaining them, and their use for treating a variety of medical disorders, e.g., osteoporosis and other disorders of bone metabolism, cancer, viral infections, and the like.Type: GrantFiled: January 15, 2004Date of Patent: April 25, 2006Assignee: The Regents of the University of CaliforniaInventors: Karl Y. Hostetler, James R. Beadle, Ganesh D. Kini
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Patent number: 7026336Abstract: Compounds of formula (I) wherein X is O, CH2, S or NH, or the moiety X—R1 is hydrogen; V is CH or N; Y is NR10R11, NR10C(Z)NR10R11, NR10COOR11 or NR10SO2R11; Ar is phenyl or a 5- or 6-membered heteroaryl ring either of which may be optionally substituted; n is 0, 1, 2, 3 or 4; and R1, R2, R3, R4, R10 and R11 have the meanings given in the description; and pharmaceutically acceptable salt thereof.Type: GrantFiled: November 20, 2000Date of Patent: April 11, 2006Assignee: SmithKline Beecham p.l.c.Inventors: David Kenneth Dean, Peter John Lovell, Andrew Kenneth Takle
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Patent number: 7022851Abstract: This application relates to monomers of the general formula (I) for the preparation of PNA (peptide nucleic acid) oligomers and provides method for the synthesis of both predefined sequence PNA oligomers and random sequence PNA oligomers: wherein R1, R2, R3, R4, R5 is independently H, halogen, C1–C4 alkyl, nitro, nitrile, C1–C4 alkoxy, halogenated C1–C4 alkyl, or halogenated C1–C4 alkoxy, wherein at least one of R1, R3, and R5 is nitro; R6 is H or protected or unprotected side chain of natural or unnatural ?-amino acid; and B is a natural or unnatural nucleobase, wherein when said nucleobase has an exocyclic amino function, said function is protected by protecting group which is labile to acids but stable to weak to medium bases.Type: GrantFiled: January 24, 2003Date of Patent: April 4, 2006Assignee: Panagene, Inc.Inventors: Sung Kee Kim, Hyunil Lee, Jong Chan Lim, Hoon Choi, Jae Hoon Jeon, Sang Youl Ahn, Sung Hee Lee
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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: 7009050Abstract: The embodiments described herein concern 5-substituted pyrimidine derivatives of conformationally locked nucleoside analogues and to the use of these derivatives as anti-viral and anti-cancer agents. The compounds are of the formula: wherein B is uracil-1-yl or cytosin-1-yl having a 5-substituent selected from halogen, alkyl, alkenyl, and alkynyl, with the proviso that where B is uracil-1-yl, the 5-substituent is not methyl. The compounds are useful in the treatment of Herpes simplex virus (HSV).Type: GrantFiled: January 15, 2003Date of Patent: March 7, 2006Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Victor E. Marquez, Pamela L. Russ
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Patent number: 7001910Abstract: The present invention refers to compounds of the general formula (I), to their possible pharmaceutically acceptable salts and tautomeric forms. The present invention also refers to a process for their production and to their use as antidiabetic and *hypoglycemic agents, alone or in combination with other antidiabetic agents, such as sulfonilureas or biguanides, as well as for the treatment of complications associated to the resistance to the insulin, such as hypertension, hyperuricemia or other cardiovascular, metabolic, endocrine conditions, or other conditions related with diabetes.Type: GrantFiled: November 15, 2000Date of Patent: February 21, 2006Assignee: Vita-Invest S.A.Inventors: Marisabel Mourelle Mancini, Juan Carlos Del Castillo Nieto, Elisabet De Ramon Amat
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Patent number: 6969766Abstract: This application relates to monomers of the general formula (I) for the preparation of PNA (peptide nucleic acid) oligomers and provides method for the synthesis of both predefined sequence PNA oligomers and random sequence PNA oligomers: wherein E is nitrogen or C—R?; J is sulfur or oxygen; R?, R1, R2, R3, R4 is independently H, halogen, alkyl, nitro, nitrile, alkoxy, halogenated alkyl, halogenated alkoxy, phenyl or halogenated phenyl, R5 is H or protected or unprotected side chain of natural or unnatural ?-amino acid; and B is a natural or unnatural nucleobase, wherein when said nucleobase has an exocyclic amino function, said function is protected by protecting group which is labile to acids but stable to weak to medium bases in the presence of thiol.Type: GrantFiled: April 25, 2003Date of Patent: November 29, 2005Assignee: Panagene, Inc.Inventors: Sung Kee Kim, Hyunil Lee, Jong Chan Lim, Hoon Choi, Jae Hoon Jeon, Sang Youl Ahn, Sung Hee Lee, Won Jun Yoon
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Patent number: 6960662Abstract: The present invention relates to a process for preparing 2-(pyridin-4-ylamino-pyrido [2,3-d]pyrimidine of Formula II by reacting a 4-aminopyridine of the formula with a 2-(4-imino-4H-pyridin-1-yl)-pyrido[2,3-d]pyrimidine of Formula I in the presence of a base. It also relates to an alternative process for preparing a compound of Formula II by reacting the aminopyridine hereinabove with in a unreactive organic solvent. It also relates to the compound of Formula III.Type: GrantFiled: July 12, 2001Date of Patent: November 1, 2005Assignee: Warner-Lambert CompanyInventors: Vladimir Genukh Beylin, Richard Jungkyu Lee, Mark Eugene Marlatt
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Patent number: 6958345Abstract: Compounds which are active against viruses have the following Formulas: wherein B is a purine or pyrimidine heterocyclic ring and is preferably selected from the group consisting of 6-aminopurine (adenine), 2,6-diaminopurine, 2-amino-6-azidopurine, 2-amino-6-cyclopropylaminopurine, 6-hydroxypurine (hypoxanthine), 2-amino-6-halo substituted purines, 2-amino-6-alkoxy substituted purines, 2-amino-6-hydroxypurine (guanine), 3-deazapurines, 7-deaza-purines, 8-azapurines, cytosine, 5-halo substituted cytosines, 5-alkyl substituted cytosines, thymine, uracil and 6-azapyrimidines; X is O; and, R1 and R2 are alkyl or aryl groups. The compounds of the present invention also include the R- and S-enantiomers of the above compounds. The R1X and/or R2X can also be amino acid residues with X as NH.Type: GrantFiled: August 6, 2004Date of Patent: October 25, 2005Assignees: The Regents of the University of Michigan, Wayne State UniversityInventors: Jiri Zemlicka, Yao-Ling Qiu, John C. Drach, Roger G. Ptak
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Patent number: 6951856Abstract: The invention relates to novel aryl-ethene-sulfonamides and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as endothelin receptor antagonists.Type: GrantFiled: July 10, 2001Date of Patent: October 4, 2005Assignee: Actelion Pharmaceuticals Ltd.Inventors: Christoph Boss, Martin Bolli, Martine Clozel, Walter Fischli, Thomas Weller
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Patent number: 6939965Abstract: Processes for the preparation of 1,3-oxathiolane nucleosides are provided that include reacting a 5-O-protected-oxymethyl-1,3-oxathiolane with a silylated nucleoside in the presence of (Cl)3Ti(isopropoxide). Using the processes described herein, the compounds can be provided as isolated enantiomers.Type: GrantFiled: February 11, 2003Date of Patent: September 6, 2005Assignees: Gilead Sciences, Inc., Emory UniversityInventors: George R. Painter, Dennis C. Liotta, Merrick R. Almond, Darryl G. Cleary, José D. Soria, Marcos Sznaidman
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Patent number: 6936602Abstract: Compounds of the general formula (I): or salts thereof, which exhibit CCR5 antagonism and exert preventive and therapeutic effects against HIV infections: wherein R1 is a 5- to 6-membered aromatic ring which bears a substituent represented by the general formula: R-Z1-X-Z2- (wherein R1 is hydrogen or optionally substituted hydrocarbyl; X is optionally substituted alkylene; and Z1 and Z2 are each a heteroatom) and may be further substituted, with R being optionally bonded to the aromatic ring to form another ring; Y is optionally substituted imino; and R2 and R3 are each optionally substituted aliphatic hydrocarbyl or an optionally Substituted hetero-alicyclic group.Type: GrantFiled: June 15, 2000Date of Patent: August 30, 2005Assignee: Takeda Chemical Industries, Ltd.Inventors: Mitsuru Shiraishi, Masanori Baba, Yoshio Aramaki, Naoyuki Kanzaki, Osamu Nishimura
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Patent number: 6933288Abstract: This invention is directed to novel pyranosyl cytosine compounds depicted graphically as structure I. This invention is further directed to a unique methodology for their preparation using solid-phase methodology. These hexopyranosyl cytosine derived natural product analogs share their parent compounds broad-spectrum antimicrobial and anti-fungal profile and represent a vast, novel compound class of 50S rRNA directed inhibitors of protein translation.Type: GrantFiled: February 4, 2002Date of Patent: August 23, 2005Assignee: ISIS Pharmaceuticals, Inc.Inventors: Michael T. Migawa, Eric E. Swayze, Richard H. Griffey
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Patent number: 6927291Abstract: An efficient synthetic route to antiviral 2?,3?-dideoxy-2?,3?-didehydro-nucleosides, such as 2?,3?-dideoxy and 2?- or 3?-deoxyribo-nucleoside analogs, from available precursors is disclosed, with the option of introducing functionality as needed. In one embodiment, a method for the preparation of ?-D and ?-L-2?,3?-dideoxy-2?,3?-didehydro-nucleosides is described that includes: activating a compound of structure (1) wherein B is a pyrimidine or purine base and Y is O, S or CH2 with an acyl halide of the formula X—C(?O)R1, X—C(?O)C(R1)2OC(?O)R1 or X—C(?O)OR1 (wherein X is a halogen, and each R1 is independently hydrogen, lower alkyl, alkyl, aryl or phenyl); reducing the resulting compound with a reducing agent to form a 2?,3?-dideoxy-2?,3?-didehydro-nucleoside; and optionally deprotecting the nucleoside. The haloacylation of the first step can form the 2?-acyl-3?-halonucleoside, the 3?-acyl-2?-halonucleoside, or a mixture thereof.Type: GrantFiled: March 1, 2002Date of Patent: August 9, 2005Assignee: Pharmasset, Ltd.Inventors: Fuqiang Jin, Pasquale N. Confalone
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Patent number: 6919346Abstract: Isoxazolone compounds having the generic structure: are used to treat disease associated with unwanted cytokine activity, including rheumatoid arthritis, osteoarthritis, diabetes, HIV/AIDS, inflammatory bowel disease, Crohn's disease, ulcerative colitis, congestive heart, hypertension, chronic obstructive pulmonary disease, septic shock syndrome, tuberculosis, adult respiratory distress, asthma, atherosclerosis, muscle degeneration, periodontal disease, cachexia, Reiter's syndrome, gout, acute synovitis, anorexia and bulimia nervosa fever, malaise, myalgia and headaches.Type: GrantFiled: December 2, 2003Date of Patent: July 19, 2005Assignee: The Procter & Gamble CompanyInventors: Michael Philip Clark, Jane Far-Jine Djung, Steven Karl Laughlin, Joshua Spector Tullis, Michael George Natchus, Biswanath De
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Patent number: 6906068Abstract: The invention relates to substituted polycyclic aryl and heteroaryl pyrimidinone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.Type: GrantFiled: May 17, 2000Date of Patent: June 14, 2005Assignee: Pharmacia CorporationInventors: Michael S. South, Ashton T. Hamme, II, William L. Neumann, Darin E. Jones
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Patent number: 6900316Abstract: A process for preparing a 2-(pyridin-4-ylamino)-pyrido[2,3-d]pyrimidine of Formula II comprising reacting a 4-aminopyridine of the formula with an alkali metal amide or hydride and a 2-alkylsulfanyl-pyrido[2,3-d]pyrimidine of Formula I wherein R1, R2, R? and R?, and aryl are as defined in the specification.Type: GrantFiled: July 12, 2001Date of Patent: May 31, 2005Assignee: Warner-Lamber CompanyInventors: Howard Isaac Tjiong, Roy Thomas Winters
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Patent number: 6897302Abstract: The invention provides a method of synthesizing ?-L-5-fluoro-2?,3?-dideoxy-2?,3?-didehydrocytidine (?-L-FD4C). The method allows for large-scale production of ?-L-FD4C in an efficient, cost-effective, and environmentally sound manner.Type: GrantFiled: April 11, 2003Date of Patent: May 24, 2005Assignee: Achillion Pharmaceuticals, Inc.Inventors: Bo Kowalczyk, Zhao Lei, Ralph M. Schure, Lisa Dunkle
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Patent number: 6870052Abstract: Patients suffering from cancer are treated by being administered a compound represented by the following formula: wherein each R individually is H or an aliphatic or aromatic acyl group; A is selected from the group consisting of wherein X is selected from the group consisting of hydrogen, fluorine, alkoxy, alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, amino, monoalkylamino, dialkylamino, cyano and nitro. The above compounds also inhibit DNA replication in mammalian cells.Type: GrantFiled: April 7, 2003Date of Patent: March 22, 2005Assignee: Southern Research InstituteInventors: John A. Secrist, III, Kamal N. Tiwari, John A. Montgomery
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Patent number: 6867205Abstract: The present invention provides compounds of formula (I) wherein R1, R2, R3, R4 and X are as defined in the specification, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with DPP IV, such as diabetes, particularly non-insulin dependent diabetes mellitus, and impaired glucose tolerance.Type: GrantFiled: February 10, 2003Date of Patent: March 15, 2005Assignee: Hoffman-La Roche Inc.Inventors: Markus Boehringer, Bernd Michael Loeffler, Jens-Uwe Peters, Matthias Steger, Peter Weiss
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Patent number: 6867210Abstract: This invention relates aryl substituted pyridines, pyrimidines, pyrazines and triazines of Formula I: or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein A1, A2, A3, R1-R4, X and Y are set in the specification. The invention is also directed to the use of compounds of Formula I for the treatment of neuronal damage following global and focal ischemia, for the treatment or prevention of neurodegenerative conditions such as amyotrophic lateral sclerosis (ALS), and for the treatment, prevention or amelioration of both acute or chronic pain, as antitinnitus agents, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.Type: GrantFiled: March 12, 2001Date of Patent: March 15, 2005Assignee: Euro-Celtique S.A.Inventors: Derk J. Hogenkamp, Phong Nguyen, Bin Shao
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Patent number: RE39056Abstract: Compounds of structural Formula (I) and pharmacologically acceptable salts and esters thereof possess 5?-reductase inhibitory activity. These compounds inhibit 5?-reductase type 1 and type 2. The compounds of structural Formula I are useful in the systemic, including oral, and parenteral, including topical, treatment and prevention of hyperandrogenic conditions including prostatic carcinoma, benign prostatic hyperplasia, acne vulgaris, seborrhea, androgenic alopecia (also called androgenetic alopecia) which includes male- and female-pattern baldness, female hirsutism, and prostatitis. A class of compounds of the present invention are also potent antiandrogens. The present invention also relates to novel compositions containing such compounds, methods of their use and methods of their manufacture.Type: GrantFiled: September 11, 1996Date of Patent: April 4, 2006Assignee: Merck & Co, Inc.Inventors: Raman K. Bakshi, Soumya P. Sahoo, Richard L. Tolman
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Patent number: RE39265Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: November 9, 2000Date of Patent: September 5, 2006Assignee: Aventis Pharmaceuticals Inc.Inventors: Joseph T. Strupczewski, Kenneth J. Bordeau, Edward J. Glamkowski, Yulin Chiang, Grover C. Helsley