Patents Examined by Thomas C. McKenzie
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Patent number: 7186831Abstract: This invention relates to novel triazolopyrimidines of the formula in which R1, R2, R3, R4and X have the meanings given in the disclosure, to a plurality of processes for preparing these novel substances, and to their use for controlling unwanted microorganisms. This invention further relates to novel intermediates of the formulae and processes for their preparation and additionally relates to novel amines and carbamates of the formulae given in the disclosure and processes for their preparation.Type: GrantFiled: April 18, 2002Date of Patent: March 6, 2007Assignee: Bayer Cropscience LPInventors: Olaf Gebauer, Jörg Nico Greul, Ulrich Heinemann, Hans-Ludwig Elbe, Bernd-Wieland Krüger, Fritz Maurer, Ralf Dunkel, Arnd Voerste, Ronald Ebbert, Ulrike Wachendorff-Neumann, Yoshinori Kitagawa, Astrid Mauler-Machnik, Karl-Heinz Kuck
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Patent number: 7169924Abstract: Compound of formula (I): are disclosed in which: R1 is an aryl group, optionally substituted by 1, 2, 3 or 4 substituents which may be the same or different selected from C(1-6)alkyl, C(1-6)alkoxy, C(1-6)alkylthio, hydroxy, halogen, CN, and mono to perfluoro-C(1-4)alkyl; R2 is halogen, C(1-3)alkyl, C(1-3)alkoxy, hydroxyC(1-3)alkyl, C(1-3)alkylthio, C(1-3)alkylsulphinyl, aminoC(1-3)alkyl, mono- or di-C(1-3)alkylaminoC(1-3)alkyl, C(1-3)alkylcarbonylaminoC(1-3)alkyl, C(1-3)alkoxyC(1-3)alkylcarbonylaminoC(1-3)alkyl, C(1-3)alkylsulphonylaminoC(1-3)alkyl, C(1-3)alkylcarboxy, C(1-3)alkylcarboxyC(1-3)alkyl, and R3 is hydrogen, halogen, C(1-3)alkyl, or hydroxyC(1-3)alkcyl; or R2 and R3 together with the pyrimidone ring carbon atoms to which they are attached form a fused 5-or 6-membered carbocyclic ring; or R2 and R3 together with the pyrimidone ring carbon atoms to which they are attached form a fused benzo or heteroaryl ring ring optionally substituted by 1, 2, 3 or 4 substituents which may be the same or difType: GrantFiled: October 5, 2001Date of Patent: January 30, 2007Assignee: SmithKline Beecham plcInventors: Richard Leonard Elliott, Deirdre Mary Bernadette Hickey, Robert John Ife, Colin Andrew Leach, Ivan Leo Pinto, Stephen Allan Smith
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Patent number: 7160894Abstract: A novel compound represented by the formula (1): [R1 represents hydrogen atom, chlorine atom, or hydroxyl group; X1 . . . X2 represents—CH(R2)—CH(R3)—, —CH(R2)—CH(R3)—CH(R4)—, etc.; R2 to R4represent hydrogen atom, or an alkyl group; A1, A11, A2, and A21 represent hydrogen atom, or an alkyl group; Y represents —CH(A3)—, —CH(A3)—C(A4)(A41)—, —CH(A3)—C(A4)(A41)—C(A5)(A51)—, or a single bond; A3, A4, A41, A5, and A51 represent hydrogen atom, or an alkyl group; Z represents hydroxyl group, or —N(A6)(A61); A6 represents hydrogen atom, or an alkyl group, A61 represents hydrogen atom, an alkyl group, an aralkyl group, etc.; and groups in each of one or more combinations selected from the group consisting of combinations of A6 and A3, A6 and A4, A6 and A1, A6 and A2, A2 and A3, A2 and A4, A6 and A5, A3 and A1, and A5 and A1 may bind to each other to form a 5- or 6-membered ring], or a salt thereof, which potently inhibits the phosphorylation of myosin regulatory light chain.Type: GrantFiled: June 3, 2004Date of Patent: January 9, 2007Assignee: Asahi Kasei Pharma CorporationInventors: Rintaro Yamada, Minoru Seto
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Patent number: 7161003Abstract: In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.Type: GrantFiled: September 3, 2003Date of Patent: January 9, 2007Assignees: Schering Corporation, Pharmacopeia Drug Discovery, Inc.Inventors: Timothy J. Guzi, Kamil Paruch, Michael P. Dwyer, Ronald J. Doll, Viyyoor M. Girijavallabhan, Alan Mallams, Carmen S. Alvarez, Kartik M. Keertikar, Jocelyn Rivera, Tin-Yau Chan, Vincent Madison, Thierry O. Fischmann, Lawrence W. Dillard, Vinh D. Tran, Zhen Min He, Ray Anthony James, Haengsoon Park, Vidyadhar M. Paradkar, Douglas Walsh Hobbs
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Patent number: 7148350Abstract: The present invention describes new homo or heterodimer prodrugs wherein both active monomeric units are compounds of the formula: where R1 and R2 are each independently —H, —C1–C6 alkyl —C1 –C6OH, or —C1–C6NHR?, wherein R? is —H, or —C1–C6 alkyl, R3 is: where R4 and R5 are defined in the description. The monomeric units are coupled to each other via a labile carbonate (—O—COO—), carbamate (—O—CO—N—), urea (—N—CO—N—) or phosphate (—O—POO—O—) moiety. Such homo or heterodimer prodrugs are useful in the treatment of erectile dysfunction.Type: GrantFiled: August 7, 2001Date of Patent: December 12, 2006Assignees: Cristalia Prod.Qui.Farm. LTDAInventors: Elisa Mannochio De Souza Russo, Valter Freire Torres Russo
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Patent number: 7135568Abstract: Substituted pyrazolopyrimidines and thiazolopyrimidines, specifically, compounds corresponding to the structure (I A), (I B) or (II) processes for their preparation, substance libraries containing them, pharmaceutical formulations containing these compounds, the use of these compounds for the production of medicaments for the treatment and/or prophylaxis of pain and related treatment methods are provided.Type: GrantFiled: September 12, 2003Date of Patent: November 14, 2006Assignee: Gruenenthal GmbHInventors: Matthias Gerlach, Corrinna Sundermann, Utz-Peter Jagusch, Bernd Sundermann, Martin Fuhr, Adriaan P. Ijzerman, Miriam Dissen-De Groote
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Triaza- and tetraaza-anthracenedione derivatives, their preparation and their use as pharmaceuticals
Patent number: 7132536Abstract: The present invention relates to triaza- and tetraaza-anthracenedione derivatives of the formula I, wherein A, B and R1 to R5 are as defined herein. The compounds of formula I are valuable pharmacologically active compounds. They are useful in the treatment of various disease states including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency. They upregulate the expression of the enzyme endothelial nitric oxide (NO) synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.Type: GrantFiled: April 21, 2004Date of Patent: November 7, 2006Assignee: Sanofi-aventis Deutschland GmbHInventors: Andreas Weichert, Hartmut Strobel, Paulus Wohlfart, Marcel Patek, Martin Smrcina, Aleksandra Weichsel -
Patent number: 7129351Abstract: Disclosed are novel pyrimido compounds that are inhibitors of Src family of tyrosine 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, hepatic and pancreatic tumors. Also disclosed are pharmaceutical compositions containing these compounds and methods of treating cancer.Type: GrantFiled: October 20, 2003Date of Patent: October 31, 2006Assignee: Hoffmann-La Roche Inc.Inventors: Kin-Chun Luk, Pamela Loreen Rossman, Stefan Scheiblich, Sung-Sau So
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Substituted amidoalkyl uracils and their use as inhibitors of the poly(adp-ribose) synthetase (PARS)
Patent number: 7125995Abstract: This application relates to compounds of formula (I) below in which the several variable groups are as defined in the specification and claims, to methods of preparing these materials, to pharmaceutical compositions containing these materials, and to methods of using these materials to treat ischaemia or reperfusion damage.Type: GrantFiled: November 2, 2001Date of Patent: October 24, 2006Assignee: Bayer AktiengesellschaftInventors: Barbara Albrecht, Michael Gerisch, Gabriele Handke-Ergüden, Axel Jensen, Thomas Krahn, Werner Nickl, Felix Oehme, Karl-Heinz Schlemmer, Henning Steinhagen -
Patent number: 7119200Abstract: In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.Type: GrantFiled: February 11, 2004Date of Patent: October 10, 2006Assignees: Schering Corporation, Pharmacopeia Drug Discovery, Inc.Inventors: Timothy J. Guzi, Kamil Paruch, Michael P. Dwyer, Ronald J. Doll, Viyyoor M. Girijavallabhan, Alan Mallams, Carmen S. Alvarez, Kartik M. Keertikar, Jocelyn Rivera, Tin-Yau Chan, Vincent Madison, Thierry O. Fischmann, Lawrence W. Dillard, Vinh D. Tran, Zhen Min He, Ray Anthony James, Haengsoon Park, Vidyadhar M. Hobbs, Douglas Walsh Hobbs
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Patent number: 7119105Abstract: The present invention relates to () non-peptide aspartyl protease inhibitors; (ii) methods for modulating the processing of an amyloid precursor protein (APP); (iii) methods for modulating the processing of a tau protein (?-protein); and (iv) methods for treating neurodegenerative diseases.Type: GrantFiled: February 5, 2004Date of Patent: October 10, 2006Assignee: The Regents of the University of CaliforniaInventors: Jonathan A. Ellman, Gary Lynch, Irwin D. Kuntz, Xiaoning Bi, Christina E. Lee, A. Geoffrey Skillman, Tasir Haque
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Patent number: 7119199Abstract: The present invention is directed to a method for producing a pyridopyrimidone of the formula wherein X is N or CH and R is an aryl, heteroaryl or alkyl group, said method comprising the step of reacting an acid derivative of the formula: wherein X is N or CH; Y is an appropriate leaving group; Z is a halogen, OR1, NHR1, or SR1; and R1 is a lower alkyl; and the amidine derivative is wherein R is an aryl, heteroaryl or alkyl group.Type: GrantFiled: December 31, 2004Date of Patent: October 10, 2006Assignee: Scios INCInventors: Sarvajit Chakravarty, Sundeep Dugar, Richland Tester, Aurelia Conte
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Patent number: 7115739Abstract: This invention describes novel triazole compounds of formula IX: wherein Z1 is nitrogen or CR9 and Z2 is nitrogen or CH, provided that at least one of Z1 and Z2 is nitrogen; G is Ring C or Ring D; Ring C is selected from a phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, or 1,2,4-triazinyl ring, wherein said Ring C has one or two ortho substituents independently selected from —R1; Ring D is a 5–7 membered monocyclic ring or 8–10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx and Ry are independently selected from T-R3, or Rx and Ry are taken together with their intervening atoms to form a fused ring; R1, R3, and T are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of GSK-3 and Aurora, for treating diseases such as diabetes, cancer, and Alzheimer's disease.Type: GrantFiled: September 14, 2001Date of Patent: October 3, 2006Assignee: Vertex Pharmaceuticals IncorporatedInventors: David Bebbington, Ronald Knegtel, Hayley Binch, Julian M. C. Golec, Pan Li, Jean-Damien Charier
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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: 7115741Abstract: Compounds of formula II are provided: wherein A, J and L are independently a direct link or a divalent linking group. The compounds are useful in the treatment of thrombosis.Type: GrantFiled: September 6, 2002Date of Patent: October 3, 2006Inventors: Daniel E. Levy, Mark S. Smyth, Robert M. Scarborough
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Patent number: 7115742Abstract: A process for the preparation of triethylenediamine (TEDA) by reaction of ethylenediamine (EDA) in the presence of a zeolite catalyst, wherein the zeolite catalyst contains one or more metals M in oxidation states II, III or IV as oxides. The desired molar ratio of SiO2 to metal oxide of the zeolite catalyst depends on the oxidation state of the metal M as specified herein. The reaction temperature is from 250 to 500° C. TEDA is an important basic chemical and is used, among other things, in the preparation of pharmaceuticals and plastics, in particular as a catalyst in the preparation of polyurethanes.Type: GrantFiled: February 6, 2003Date of Patent: October 3, 2006Assignee: BASF AktiengesellschaftInventors: Matthias Frauenkron, Bernd Stein
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Patent number: 7115738Abstract: Compounds are described and claimed comprising general formula: The compounds have substituents as described herein and are useful, e.g., for their ability to bind nucleic acids and thereby effect purifications, probing techniques and gene inhibition.Type: GrantFiled: March 13, 2001Date of Patent: October 3, 2006Assignee: Active MotifInventors: Vladimir Efimov, Joseph Fernandez, Dorothy Archdeacon, John Archdeacon, Oksana Chakhmakhcheva, Alla Buryakova, Mikhail Choob, Kyle Hondorp
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Patent number: 7112676Abstract: Disclosed are novel pyrimido compounds that are selective inhibitors of both KDR and FGFR kinases and are selective against LCK. 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: October 20, 2003Date of Patent: September 26, 2006Assignee: Hoffmann-La Roche Inc.Inventors: Apostolos Dermatakis, Marek Michal Kabat, Kin-Chun Luk, Pamela Loreen Rossman, Sung-Sau So
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Patent number: 7109331Abstract: The present invention provides a compound of the formula (I): wherein A is selected from N, CH and CR, where R is selected from halogen, optionally substituted alkyl, aralkyl and aryl, OH, NH2, NHR1, NR1R2 and SR3, where R1, R2 and R3 are each optionally substituted alkyl, aralkyl or aryl groups; B is selected from OH, NH2, NHR4, H and halogen, where R4 is an optionally substituted alkyl, aralkyl or aryl group; D is selected from OH, NH2, NHR5, H, halogen and SCH3, where R5 is an optionally substituted alkyl, aralkyl or aryl group; X and Y are independendy selected from H, OH and halogen, with the proviso that when one of X and Y is hydroxy or halogen, the other is hydrogen; Z is OH, or, when X is hydroxy, Z is selected from hydrogen, halogen, hydroxy, SQ and OQ, where Q is an optionally substituted alkyl, aralkyl or aryl group; and W is OH or H, with the proviso that when W is OH, then A is CR where R is as defined above; or a tautomer thereof; or a pharmaceutically acceptable salt thereof; or an ester tType: GrantFiled: August 24, 2001Date of Patent: September 19, 2006Assignees: Industrial Research Limited, Albert Einstein College of Medicine of Yeshiva UniversityInventors: Richard Hubert Furneaux, Peter Charles Tyler, Vern L. Schramm
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Patent number: 7109332Abstract: 2,4-Dioxo-3-quinazolinylaryl sulfonylurea compounds having the formula: wherein R is a member selected from the group consisting of H and C1-6 alkyl; R1 is a member selected from the group consisting of H, C1-6 alkyl, C1-6 haloalkyl, C3-5 cycloalkyl and C3-5 cycloalkyl-alkyl; R2 is a member selected from the group consisting of H, halogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C1-6 alkoxy, cyano and —C(O)R2a, wherein R2a is a member selected from the group consisting of C1-6 alkoxy and (C1-6 alkyl)0-2 amino; L is a 1 to 3 carbon linking group selected from the group consisting of —CH2—, —CH(CH3)—, —CH2CH2—, —CH2CH(CH3)— and —CH2CH2CH2—; L1 is a linking group selected from the group consisting of a bond and —CH2—; L2 is a linking group selected from the group consisting of a bond, —NH— and —CH2—; and Ar1 is an aromatic ring selected from the group consisting of benzene, pyridine and pyrimidine; are provided.Type: GrantFiled: September 29, 2004Date of Patent: September 19, 2006Assignee: Portola Pharmaceuticals, Inc.Inventors: Robert M. Scarborough, Wolin Huang, Anjali Pandey, Shawn M. Bauer, Xiaoming Zhang, Zhaozhong J. Jia