Pyrimidinecarboxamide derivatives and their use as...

Details Pyrimidinecarboxamide derivatives and their use as... Pyrimidinecarboxamide derivatives and their use as...

2007-02-13

2007-02-13

Wilson, James O. (Department: 1621)

Organic compounds -- part of the class 532-570 series

Organic compounds

Four or more ring nitrogens in the bicyclo ring system

C544S243000, C544S245000, C544S246000, C544S247000, C544S249000, C544S294000, C544S295000

Reexamination Certificate

active

10407870

ABSTRACT:
This invention is directed to compound of the following formula (I):wherein R1, R2, R3and R4are as described herein. These compounds and pharmaceutical compositions containing the compounds are useful in treating inflammatory disorders in mammals.

REFERENCES:
patent: 3821225 (1974-06-01), Regnier et al.
patent: 3845055 (1974-10-01), Hoegerle et al.
patent: 3970661 (1976-07-01), Regnier et al.
patent: 3970663 (1976-07-01), Regnier et al.
patent: 4285946 (1981-08-01), Kampe et al.
patent: 4410530 (1983-10-01), Frei et al.
patent: 4705792 (1987-11-01), Granzer et al.
patent: 4734418 (1988-03-01), Yokoyama et al.
patent: 5654307 (1997-08-01), Bridges et al.
patent: 5665724 (1997-09-01), Sanfilippo et al.
patent: 5756524 (1998-05-01), Riordan et al.
patent: 5939424 (1999-08-01), Böger et al.
patent: 6432963 (2002-08-01), Hisamichi et al.
patent: 6656935 (2003-12-01), Yamada et al.
patent: 6759412 (2004-07-01), Strobel et al.
patent: 2003/0032647 (2003-02-01), Yamada et al.
patent: 2405930 (1975-08-01), None
patent: EP 0 569 912 (1993-11-01), None
patent: 0 569 912 (1993-11-01), None
patent: 0 626 428 (2000-10-01), None
patent: 1 223 170 (2002-07-01), None
patent: 1 277 741 (2003-01-01), None
patent: 1131784 (1968-10-01), None
patent: 49076886 (1974-07-01), None
patent: 61087672 (1986-05-01), None
patent: 01117882 (1989-05-01), None
patent: 03127790 (1991-05-01), None
patent: WO 01/021615 (2001-03-01), None
patent: WO 95/19774 (1995-07-01), None
patent: WO 95/25723 (1995-09-01), None
patent: WO 99/06035 (1999-02-01), None
patent: WO 99/06046 (1999-02-01), None
patent: WO 99/61444 (1999-12-01), None
patent: WO 99/66925 (1999-12-01), None
patent: WO 00/39101 (2000-07-01), None
patent: WO 01/21597 (2001-03-01), None
patent: WO 01/44213 (2001-06-01), None
patent: WO 01/74788 (2001-10-01), None
patent: WO 02/04429 (2002-01-01), None
patent: WO 02/066036 (2002-08-01), None
Kosegi et al., “Preparation of N-(1H-Tetrazol-5-yl)-2-anilino-5-pyrimidinecarboxamide Derivatives as Antiallergic and Antiulcer Agents”,Chemical Abstracts Database, Accession No. 1991:583346, 1989. Abstract corresponds to entry BM below.
“(Amidoethyl)piperazines,”Chemical Abstracts Database, Accession No. 1976:463091, 1972. Corresponds to entry BO above.
Regnier, et al., “N-Amidoethyl Piperazines,”Chemical Abstracts Database, Accession No. 1976:446755, 1976.
Kon et al., “Preparation of Heterocyclic Carboxamides as Digestive Tract Motility Stimulants,”Chemical Abstracts Database, Accession No. 1989:632842. Corresponds to entry BQ above.
Shimizu et al., “High-performance Affinity Beads for Identifying Drug Receptors”,Nature Biotechnology(Aug. 2000), vol. 18, pp. 877-881.
Sheikh, S. P. et al., “Binding of Monoiodinated Neuropeptide Y to Hippocampal Membranes and Human Neuroblastoma Cell Lines”,The Journal of Biological Chemistry(Apr. 29, 1989), vol. 264, pp. 6648-6654.
Fuhlendorff, J. et al., “[Leu31,Pro34]Neuropeptide Y: A Specific Y1Receptor Agonist”,Proceedings of the National Academy of Sciences USA(Jan. 1990), vol. 87, pp. 182-186.
Samson, M. et al., “The Second Extracellular Loop of CCR5 Is the Major Determinant of Ligand Specificity”,The Journal of Biological Chemistry(Oct. 3, 1997), vol. 272, pp. 24934-24941.
Ahuja, S. K. et al., “The CXC Chemokines Growth-regulated Oncogene (GRO) α, GROβ, GROγ, Neutrophil-activating Peptide-2, and Epithelial Cell-derived Neutrophil-activating Peptide-78 Are Potent Agonists for the Type B, but Not the Type A, Human Interleukin-8 Receptor”,The Journal of Biological Chemistry(Aug. 1996), vol. 271, pp. 20545-20550.
Frei et al., “Heterocyclic compounds”,Chemical Abstracts Database, Accession No. 1974:535967, 1974. Abstract corresponds to entry BK above.
Urleb, U. et al., “Transformations of 2,4,5-Trisubstituted Pyrimidines. The Syntheses and Transformations of Pyrimido/4,5-d/Pyrimidine, 1,2,4-Triazolo/4,3-a/Pyrimidine, Tetrazolo/1,5-a/Pyrimidine, 1,2,4-Triazolo/3,4-bPurine and Tetrazolo/5,1-b/Purine Derivatives”,Heterocycles(1986), vol. 24, pp. 1899-1909.
Kim, D. H., “Reactions of Ethyl 4-Chloro-5-pyrimidinecarboxylates with 2-Aminopyridine. Synthesis of 5H-Pyrido[1,2-a]pyrimido[5,4-e]pyrimidin-5-ones and 5H-Pyrido[1,2-a]pyrimido[4,5-d]pyrimidin-5-ones and Rearrangement of the Former to the Latter”,Journal of Heterocyclic Chemistry(Jan./Feb. 1985), vol. 22, pp. 173-176.
Huettinger, M. et al., “Hypolipidemic Activity of HOE-402 Is Mediated by Stimulation of the LDL Receptor Pathway”,Arteriosclerosis and Thrombosis(1993), vol. 13, pp. 1005-1012.
Hoffman, A. et al., “Cholesterol Lowering Action of HOE 402 in the Normolipidemic and Hypercholesterolemic Golden Syrian Hamster”,Biochimica et Biophysica Acta(1996), vol. 1299, pp. 95-102.
Gupta, S.P., “Potential Anticancer Agents: Synthesis of Cytidine-5-carboxylic Acid and Cytosine-5-carbonylaminoacids”,Indian Journal of Chemistry, (1976), vol. 15B, pp. 463-465.
Rosania, G. R., “Myoserverin, A Microtubule-binding Molecule with Novel Cellular Effects”,Nature Biotechnology(2000), vol. 18, pp. 304-308.
Fleming, S. A., “Chemical Reagents in Photoaffinity Labeling”,Tetrahedron(1995), vol. 51, pp. 12479-12520.
Srikant, C. B., “Relationship between Receptor Binding and Biopotency of Somatostatin-14 and Somatostatin-28 in Mouse Pituitary Tumor Cells”,Endocrinology(Jul. 1985), vol. 117, pp. 271-278.
Katsuragi, T. et al., “Affinity Chromatography of Cytosine Deaminase fromEscherichia coliwith Immobilized Pyrimidine Compounds”,Agricultural and Biological Chemistry(Jul. 1986), vol. 50, pp. 1713-1719.
Thermos, K. et al., “Somatostatin Receptor Subtypes in the Clonal Anterior Pituitary Cell Lines AtT-20 and GH3”,Molecular Pharmacology(Apr. 1988), vol. 33, pp. 370-377.
Takayama, et al., “Preparation of Benzimidazole Derivatives as Poly(ADP-ribose) Polymerase (PARP) Inhibitors”,Chemical Abstracts Database, Accession No. 2001: 228885, 2000. Abstract corresponds to entry BP above.
Stogryn, E. L., “Synthesis of Trimethoprim Variations. Replacement of CH2by Polar Groupings”,Journal of Medicinal Chemistry(1972), vol. 15, pp. 200-201.
Kamath, S. et al., “Calculation of Relative Binding Free Energy Difference of DHFR Inhibitors by a Finite Difference Thermodynamic Integration (FDTI) Approach”,Journal of Biomolecular Structure&Dynamics(1999), vol. 16, pp. 1239-1244.
Dostert, R. et al., “Studies On the Neuroleptic Benzamides”,European Journal of Medicinal Chemistry—Chimie Thérapeutique(1982), vol. 17, pp. 437-444.
Hirota, K. et al., “Novel Ring Transformations of 5-Cyanouracils into 2-Thiocytosines, 2,4-Diaminopyrimidines, and Pyrimido[4,5-d]pyrimidines by the Reaction with Thioureas and Guanidines”,Journal of the Chemical Society, Perkin Transactions I(1990), vol. 1, pp. 123-128.
Karlsson, R. et al., “Biosenser Analysis of Drug-Target Interactions: Direct and Competitive Binding Assays for Investigation of Interactions Between Thrombin and Thrombin Inhibitors”,Analytical Biochemistry(2000), vol. 278, pp. 1-13.
Kampe, K. D., “2-Cyano-3-ethoxyacrylamides—Selective Reactive Synthons for Synthesis of Heterocyclics”, abstract provided fromChemical Abstracts Database, Accession No. 1982:509955. See alsoAngewandte Chemie(1982), vol. 94, pp. 543-544.
Regnier, G. L., “Bronchodilator Substances. I. Synthesis and Structure-activity Relationships Between New Benzoic and Heterocyclic Amide Derivatives”, abstract provided fromChemical Abstracts Database, Accession No. 1975:112035. See alsoArzneimittel-Forschung(1974), vol. 24, pp. 1964-1970.
Hoffman, A. et al., “Cholesterol Lowering Potency of HOE 402 in the Hypercholesterolemic Golden Syrian Hamster”,Adv. Lipoprotein Atheroscler. Res. Diagn, Treat., Proc. Int. Dresden Lipid Symp., 8th

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