5-aminopyrazoles useful as tyrosine kinase inhibitors

Details 5-aminopyrazoles useful as tyrosine kinase inhibitors 5-aminopyrazoles useful as tyrosine kinase inhibitors

1997-04-22

1999-07-13

Richter, Johann

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

514407, 546279, 5483641, 5483657, 5483717, A61K 31415, C07D23112, C07D40106

Patent

active

059227419

ABSTRACT:
Compounds of general formula (1) are described: ##STR1## wherein Ar is an optionally substituted aromatic or heteroaromatic group;

REFERENCES:
patent: 3947467 (1976-03-01), Verge et al.
patent: 4012495 (1977-03-01), Schmiechen et al.
patent: 4015017 (1977-03-01), Gazave
patent: 4153713 (1979-05-01), Huth et al.
patent: 4193926 (1980-03-01), Schmiechen et al.
patent: 4303649 (1981-12-01), Jones
patent: 4788195 (1988-11-01), Torley et al.
patent: 4792561 (1988-12-01), Walker et al.
patent: 4876252 (1989-10-01), Torley et al.
patent: 4897396 (1990-01-01), Hubele
patent: 4921862 (1990-05-01), Walker et al.
patent: 4966622 (1990-10-01), Rempfler et al.
patent: 4971959 (1990-11-01), Hawkins
patent: 5124455 (1992-06-01), Lombardo
patent: 5128358 (1992-07-01), Saccomano et al.
patent: 5159078 (1992-10-01), Rempfler et al.
patent: 5175167 (1992-12-01), Zipperer et al.
patent: 5177085 (1993-01-01), Naef
patent: 5236918 (1993-08-01), Amschler et al.
patent: 5274002 (1993-12-01), Hawkins
patent: 5298511 (1994-03-01), Waterson
patent: 5326898 (1994-07-01), Chandraratna
patent: 5340827 (1994-08-01), Beeley et al.
patent: 5491147 (1996-02-01), Boyd et al.
patent: 5521184 (1996-05-01), Zimmermann
patent: 5550137 (1996-08-01), Beeley et al.
patent: 5580888 (1996-12-01), Warrellow et al.
patent: 5593997 (1997-01-01), Dow et al.
patent: 5608070 (1997-03-01), Alexander et al.
patent: 5622977 (1997-04-01), Warrellow
patent: 5693659 (1997-12-01), Head et al.
patent: 5723460 (1998-03-01), Warrellow et al.
patent: 5739144 (1998-04-01), Warrellow et al.
Chemical Abstracts, "Hypoglycemic Pharmaceuticals Containing Manzammide Derivatives", Chem. Abstr., 1983, 99(6), No. 43558Z.
Dent et al., "Inhibition of eosinophil cyclic nucleotide PDE activity and opsonised zymosan-stimulated respiratory burst by 'type IV'-selective PDE inhibitors", Br. J. Pharmacol., 1991, 103, 1339-1346.
Grammaticakis, "Contribution A L'Etude de L'Absortion Dans L'Ultraviolet Moyen Et Le Visible Des N-Aroyl-Arylamines. IV. 2,3-,3,4-et 2,4-, dimethoxybenzoylarylamines", Bulletin DeLa Societa Chemique De France, 1965, 848-858.
Heaslip et al., "Phosphodiesterase-IV Inhibition, Respiratory Muscle Relaxation and Bronchodilation by WAY-PDA-641", J. Pharm. Exper. Ther., 1993, 268(2), 888-896.
Karlsson et al., "T-Lymphocyte and Inflammatory Cell Research in Asthma", Joller, G. et al. (eds.), Academic Press, 1993, 323-347.
Mathison et al., "Synthesis and Hypotensive Properties of Tetrahydroixoquinolines", J. Med. Chem., 1973, 16(4), 332-336.
Miyaura, N. et al., "The Palladium-Catalyzed Cross-Coupling Reaction of Phenylboronic Acid with Haloarenes in the Presence of Bases", Synth. Comm., 1981, 11, 513-519.
Takeuchi, I. et al., "On the Antimocrobial Activity and Syntheses of Carbanilide and Salicylanilide Derivatives", Chem. Abstr., 1983, 98, No. 125577y.
Trost and Fleming (eds.), Comprehensive Organic Synthesis, Pergamon Press, New York, 1991, 3, 531-541.
Ashton, "Selective Type IV Phosphodiesterase Inhibitors as Antiasthmatic Agents. The Syntheses and Biological Activities of 3-(Cyclopentyloxy)-4-methyoxybenzamides and Analogues", J. Med. Chem., 1994, 37, 1696-1703.
Beavo & Reifsnyder, "Primary Sequence of Cyclic Nucleotide Phosphodiesterase Isozymes and the Design of Selective Inhibitors" TIPS, 1990, 11, 150-155.
Buu-Hoi, N.P. et al., "Bromination of Some 1,2,2-Triarylethylenes" J. of Organic Chemistry, 1958, 1261-1263.
Buu-Hoi et al., "New Method for the Synthesis of .omega.,.omega.-Diarylacetophenones Aminated in the Aromatic Nucleus. Plynitration of Triarylethylenes", Chem. Abstr., 1964, 61(13), 16006h.
Chan, A.C. et al., "The Role of Protein Tyrosine Kinases and Protein Tyrosine Phosphatases in T Cell Antigen Receptor Signal Transduction", Annu. Rev. Immunol., 1994, 12, 555-592.
Daves, G.D. et al., "Pyrimidines. XIII. 2-and 6-Substituted 4-Pyrimidinecarboxylic Acids", J. Of Hev. Chem., 1964, 1, 130-133.
Dietl, F. et al., "Chinone von Benzo-und Dibenzokronenethern", Synthesis, 1985, 626-631.
El-Wakil et al., "Study of the proton magnetic resonance of methoxytamoxifen towards ortho-substitiution", Chem. Abstr., 1992, 116, 255248t.
Geissler, J.F. et al., "Thiazolidine-Diones. Biochemical and Biological Activity of a Novel Class of Tyrosine Protein Kinase Inhibitors", J. Of Biol. Chem., 1990, 265(36), 22255-22261.
Hanks, S.K. et al., "The eukaryotic protein kinase superfamily: kinase (catalytic) domain structure and classification", FASEB J., 1995, 9, 576-596.
Hirose et al., "Styrene Derivatives and Electrophotographic Photoreceptor Containing Them", Chem. Abstr., 1993, 118, 136183z.
Ishikura, M. et al., "An Efficient Synthesis of 3-Heteroarylpyridines via Diethyl-(3-pyridyl)-borane" Synthesis, 1984, 936-938.
Iwashita, S. et al., "Signal Transduction System for Growth Factor Receptors Associated with Tyrosine Kinase Activity: Epidermal Growth Factor Receptor Singalling and Its Regulation", Cellular Signalling, 1992, 4(2), 123-132.
Lisle, H. et al., "IL-2-Induced Eosinophilia in the Rat Pleural Cavity: The Effect of Dexamethasone and Indomethacin", Br. J. Pharmacol. 1993, 108, 230.
Livi et al., "Cloning and Expression of cDNA for a Human Low-K.sub.m 3 Rolipram-sensitive Cyclic AMP Phosphodiesterase", Molecular and Cellular Biol. 1990, 10(6), 2678-2686.
Manhas et al., "heterocyclic Compounds XII. Quinazoline Derivatives as Potential Antifertility Agents (1)" J. Heterocyclic Chem., 1979, 16, 711-715.
Meyers, A.J. et al., "Oxazolines. XI. Synthesis of Functionalized Aromatic and Aliphatic Acids. A Useful Protecting Group for Carboxylic Acids Against Grignard and Hydride Reagents", J. Org. Chem. 1974, 39(18), 2787-2793.
Mezheritskaya, "Synthesis and properties of carboxonium het=erocyclic systems. VII. Synthesis and properties of 2-benzyl-substituted 1,3-dioxolanium salts", Chem. Abstr., 1980, 93, 95160j, 635.
Mitsunobu, O., "The Use of Diethyl Azodicarboxylate and Triphenylphosphine in Synthesis and Transformation of Natural Products" Synthesis, 1981, 1-28.
Newton, A.C., "Protein Kinase C: Structure, Function, Regulation", J. Biol. Chem., 1995, 270(48), 28495-28498.
Nicholson et al., "Differential Modulation of Tissue Function and Therapeutic Potential of Selective Inhibitors of Cyclic Nucleotide Phosphodiesterase Isoenzymes" TIPS, 1991, 12, 19-27.
O'Connor et al., "Voltammetry and Controlled Potential Oxidation of 3,4-dimethoxypropenylbenzene at a rotating platinum electrode in unbuffered acetonitrile and in acetonitrile-pyridine solution" Chem. Abstr., 1964, 60(8) #10203.4.
Ohtani, Y. et al., "Studies on Pitch Problems Caused by Pulping and Bleaching of Tropical Woods. XIV. Chemistry of the Aurone Derivatives at the Conventional Bleaching Stages", Acta Chem. Scand., 1982, 613-621.
Pines, J., "Cyclins and cyclin-dependent kinases: take your partners", TIBS, 1993, 18, 195-197.
Ple, N. et al., "Metalation of Diazines. XI. Directed Ortho-Lithiation of Fluoropyrimidines and Application to Synthesis of an Azacarboline", J. Heterocylic Chem., 1994, 31, 1311-1315.
Porter et al., "Preparation of 6-phenyl-3-(5-tetrazolyl)pyridin-=2 (H)-one Derivatives as Cyclic AMP-dependent Protein Kinase Agonists" Chem. Abstr., 1992, 117(9), 90296n.
Ramalingam, Deshmukh and Sattur, "Synthesis and Pharmacology of 2,5-Disubstituted 1,3,4-Zxadiazoles" J. Indian Chem. Soc., 1981, 58(3), 269-271.
Reddy et al., "Inhibition of Breast Cancer Cell Growth in Vitro by a Tyrosine Kinase Inhibitor" Cancer Research, 1992, 52, 3636-3641.
Sanchez, H.I. et al., "Formal Total Synthesis of .beta.-Pipitzol", Tetrahedron, 1985, 41(12), 2355-2359.
Schneider et al., "Catechol Estrogens of the 1,1,2-Triphenylbut-1-ene Type: Relationship Between Structure, Estradiol Receptor Affinity, Estrogenic and Antiestrogenic Properties, and Mammary Tumor Inhibiting Activities" J. Med. Chem., 1986, 29, 1355-1362.
Seitz et al., "Fluorotamoxifen. A Caveat on the Generality of Electrophilic Destannylation" Chem. Abstr., 1989, 111, 57133k.
Sharp, M.J. et al., "Synthetic Connections to the Aromatic Directed Metalation Reaction. Functionalized Aryl Boronic Acids by Ipso Borodesilylation; General Synthesis o

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