- Synthesis and pesticidal activities of 5-(2-cyclopropylaminopyrimidin-4-yl)-4-(thiophenyl)thiazole derivatives
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Pesticidal activities of 4-[5-(2-cyclopropylaminopyrimidin-4-yl)-4-(4-chloro-2-fluoro-phenyl)thiazol-2-yl]-1-methylpiperidine, designated as Comp I, have been determined against a mosquito larva, Culex pipiens pallens, and a phytopathogenic fungus, Phytophthora capsici. Comp I was used as the leading compound in this study. The compounds were synthesized by reacting them with two functional groups, 3-thiophenyl and 2-thiophenyl groups, instead of 4-chloro-2-fluorophenyl group in Comp I. Other functional groups such as 2-aminothiazole, 2-(1-methylpiperazin-4-yl)thiazole, and 2-(piperazin-4-yl)thiazole were also introduced instead of 2-methylpiperidin-4-yl-thiazole of Comp I. Compounds designated as XIII-6XV-7 were newly synthesized and their structures were confirmed by 1H- and 13C-NMR spectroscopy. Mosquito larvicidal activities of all the synthesized compounds against C. pipiens pallens were examined and Comp I among them showed the strongest larvicidal activity as 0.513 mM of LC50 value. The fungicidal activities of all the synthesized compounds against P. capsici were examined using the whole plant method. Among the XIII-6XV-7 chemicals, 5-(2-cyclopropylaminopyrimidin-4-yl)-4-(thiophen-2-yl)thiazol-2-amine (VIII-6) showed the most potent antifungal activity in vivo. While the EC50 value of the commercial fungicide dimethomorph was 4.26 ??M, EC50 of VIII-6 was 0.94 ??M. Therefore, thiazole derivatives can be considered as viable candidates for the control of mosquito larvae and plant diseases.
- Choi, Won-Sik,Nam, Seok-Woo,Kim, Il-Doo,Kim, Seung-Han,Park, Kun-Ho,Bae, In-Kyung,Park, Eun-Sil,Jeon, Hwang-Ju,Lee, Sung-Eun
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- Design, synthesis, and in vitro antiproliferative and kinase inhibitory effects of pyrimidinylpyrazole derivatives terminating with arylsulfonamido or cyclic sulfamide substituents
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A novel series of substituted pyrimidine compounds bearing N-phenylpyrazole and terminating with aryl and cyclic sulfonamido moiety were designed, synthesized, and evaluated in vitro as antiproliferative agents against a panel of 53 cell lines of differen
- Gamal El-Din, Mahmoud M.,El-Gamal, Mohammed I.,Abdel-Maksoud, Mohammed S.,Yoo, Kyung Ho,Baek, Daejin,Choi, Jungseung,Lee, Huiseong,Oh, Chang-Hyun
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p. 111 - 122
(2016/12/14)
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- THIAZOLE AND OXAZOLE KINASE INHIBITORS
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The present invention provides thiazole and oxazole compounds, compositions containing the same, as well as processes for the preparation and methods for their use as pharmaceutical agents.
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Page/Page column 264
(2009/07/17)
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- Chemically enabled synthesis of 2-amino-4-heteroarylpyrimidines
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2-Amino-4-heteroarylpyrimidines were initially synthesized by microwave-induced SNAr reactions of primary alkyl amines and 2-methylsulfonylpyrimidines or 2-chloropyrimidines. Following this methodology, pendant piperidine functionality was elab
- Humphries, Paul S.,Do, Quyen-Quyen T.,Wilhite, David M.
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scheme or table
p. 2552 - 2554
(2009/08/09)
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- Synthesis and SAR of 4-substituted-2-aminopyrimidines as novel c-Jun N-terminal kinase (JNK) inhibitors
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The development of a series of novel 4-substituted-2-aminopyrimidines as inhibitors of c-Jun N-terminal kinases is described. The synthesis, in vitro inhibitory values for JNK1, and the in vitro inhibitory value for a c-Jun cellular assay are discussed. O
- Humphries, Paul S.,Lafontaine, Jennifer A.,Agree, Charles S.,Alexander, David,Chen, Ping,Do, Quyen-Quyen T.,Li, Lilian Y.,Lunney, Elizabeth A.,Rajapakse, Ranjan J.,Siegel, Karen,Timofeevski, Sergei L.,Wang, Tianlun,Wilhite, David M.
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scheme or table
p. 2099 - 2102
(2009/12/03)
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- PYRAZOLE COMPOUNDS
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The present invention is directed to compounds of Formula (I) and to pharmaceutically acceptable salts thereof, their synthesis, and their use as Raf inhibitors.
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Page/Page column 40; 57
(2009/03/07)
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- Synthesis and biological evaluation of trisubstituted imidazole derivatives as inhibitors of p38α mitogen-activated protein kinase
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A series of trisubstituted imidazole derivatives containing a 4-fluorophenyl group, a pyrimidine ring, and a CN- or CONH2-substituted benzyl moiety have been synthesized and evaluated for p38α MAP kinase inhibitory activity. Among them, compounds 22c, 27b, and 28b inhibited p38α MAP kinase with IC50 values 27.6, 28, and 31 nM, respectively.
- Kim, Dae-Kee,Lim, Jin-Hwi,Lee, Jung A.,Dewang, Purushottam M.
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scheme or table
p. 4006 - 4010
(2009/04/06)
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- PYRIMIDINYL-PYRAZOLE INHIBITORS OF AURORA KINASES
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The present invention provides a compound represented by Formula (I): or a pharmaceutically acceptable salt thereof, or a solvate thereof, or a combination thereof, wherein the substituents are as defined herein. The present invention also relates to a co
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Page/Page column 31
(2010/11/26)
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- Synthesis and biological activity of imidazopyridine anticoccidial agents: Part I
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Coccidiosis is the major cause of morbidity and mortality in the poultry industry. Protozoan parasites of the genus Eimeria invade the intestinal lining of the avian host causing tissue pathology, poor weight gain, and in some cases mortality. Resistance
- Scribner, Andrew,Dennis, Richard,Hong, Jean,Lee, Shuliang,McIntyre, Donald,Perrey, David,Feng, Dennis,Fisher, Michael,Wyvratt, Matthew,Leavitt, Penny,Liberator, Paul,Gurnett, Anne,Brown, Chris,Mathew, John,Thompson, Donald,Schmatz, Dennis,Biftu, Tesfaye
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p. 1334 - 1357
(2008/09/17)
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- HETEROCYCLIC COMPOUNDS
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New compounds of formula (I), wherein the meanings for the various substituents are as disclosed in the description. These compounds are useful as p38 kinase inhibitors.
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Page/Page column 44
(2008/06/13)
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- MODULATORS OF HCV REPLICATION
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The present invention is directed to the use of certain 2,4,5-trisubstituted imidazole derivatives in modulating the replication of Hepatitis C virus RNA and/or virus production in cells.
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Page/Page column 7
(2008/06/13)
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- Synthesis and SAR studies of very potent imidazopyridine antiprotozoal agents
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Compounds 10a (IC50 110 pM) and 21 (IC50 40 pM) are the most potent inhibitors of Eimeria tenella cGMP-dependent protein kinase activity reported to date and are efficacious in the in vivo antiparasitic assay when administered to chi
- Biftu, Tesfaye,Feng, Dennis,Fisher, Michael,Liang, Gui-Bai,Qian, Xiaoxia,Scribner, Andrew,Dennis, Richard,Lee, Shuliang,Liberator, Paul A.,Brown, Chris,Gurnett, Anne,Leavitt, Penny S.,Thompson, Donald,Mathew, John,Misura, Andrew,Samaras, Samantha,Tamas, Tamas,Sina, Joseph F.,McNulty, Kathleen A.,McKnight, Crystal G.,Schmatz, Dennis M.,Wyvratt, Matthew
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p. 2479 - 2483
(2007/10/03)
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- Synthesis and SAR of 2-(4-fluorophenyl)-3-pyrimidin-4-ylimidazo[1,2-a]pyridine derivatives as anticoccidial agents
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Compounds 10a-10d and 10i are very potent inhibitors of Eimeria tenella cGMP-dependent protein kinase (0.081-0.32 nM) and are very efficacious antiparasitic agents in vivo when administered to chickens at 12.5-25 ppm levels in the feed.
- Feng, Dennis,Fisher, Michael,Liang, Gui-Bai,Qian, Xiaoxia,Brown, Chris,Gurnett, Anne,Leavitt, Penny Sue,Liberator, Paul A.,Mathew, John,Misura, Andrew,Samaras, Samantha,Tamas, Tamas,Schmatz, Dennis M.,Wyvratt, Matthew,Biftu, Tesfaye
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p. 5978 - 5981
(2007/10/03)
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- Inhibitors of hepatitis C virus RNA-dependent RNA polymerase, and compositions and treatments using the same
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The invention relates to compounds of the formula 1 and to pharmaceutically acceptable salts, solvates, prodrugs and metabolites thereof, wherein W, Z, R1 and R2, are as defined herein. The invention also relates to methods of treating Hepatitis C virus in mammals by administering the compounds of formula 1, and to pharmaceutical compositions for treating such disorders, which contain the compounds of formula 1. The invention also relates to methods of preparing the compounds of formula 1.
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Page/Page column 210
(2008/06/13)
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- SUBSTITUTED IMIDAZOLES HAVING CYTOKINE INHIBITORY ACTIVITY
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Compounds represented by formula I: I are disclosed. AR represents an aromatic group containing 6-10 atoms; and represents a 4 to 10 membered non-aromatic heterocycle containing at least one N atom, and optionally containing 1-2 additional
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Page/Page column 27
(2010/02/11)
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- ISOXAZOLES AND THEIR USE IN THE TREATMENT OF ISCHEMIC DISEASES
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The present invention provides a compound of formula I, or a pharmaceutically acceptable salt thereof. These compounds are useful for the treatment of neurological, neurodegenerative, ischemic and inflammatory disorders. Accordingly, 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 neurological, neurodegenerative, ischemic and inflammatory disorders.
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Page 9-10; 18
(2010/02/06)
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- INHIBITORS OF HEPATITIS C VIRUS RNA-DEPENDENT RNA POLYMERASE, AND COMPOSITIONS AND TREATMENTS USING THE SAME
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The invention relates to compounds of the formula (I) and to pharmaceutically acceptable salts, solvates, prodrugs and metabolites thereof, wherein W, Z, R1and R2, are as defined herein. The invention also relates to methods of treating Hepatitis C virus in mammals by administering the compounds of formula (I), and to pharmaceutical compositions for treating such disorders, which contain the compounds of formula (I). The invention also relates to methods of preparing the compounds of formula (I).
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Page 428-429
(2008/06/13)
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- SUBSTITUTED HETEROCYCLIC COMPOUNDS AND METHODS OF USE
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The present invention relates to compounds having the general formula [I] or a pharmaceutically acceptable salt thereof. Also included is a method of treatment of inflammation, rheumatoid arthritis, Pagets disease, osteoporosis, multiple myeloma, uveititi
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- PYRAZOLOPYRIDINE DERIVATES
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New compounds of formula (I) and the salts, solvates and prodrugs thereof, wherein the meanings for the various substituents are as disclosed in the description. These compounds are useful as p38 kinase inhibitors.
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- PHENYL-[4-(3-PHENYL-1H-PYRAZOL-4-YL)-PYRIMIDIN-2-Yl)-AMINE DERIVATIVES
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The invention relates to phenyl-[4-(3-phenyl-1H-pyrazol-4-yl)-pyrimidin-2-yl)-amine derivatives and to processes for the preparation thereof, to pharmaceutical compositions comprising such derivatives and to the use of such derivatives - alone or in combination with one or more other pharmaceutically active compounds - for the preparation of pharmaceutical compositions for the treatment especially of a proliferative disease, such as a tumour.
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- PYRAZOLOPYRIMIDINE AND PYRAZOLOTRIAZINE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
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The present invention provides compounds of formula (I), pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceutical agents. For the prophylaxis or treatment of a condition or disease associated with a herpes viral infection.
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Page/Page column 80
(2010/02/07)
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- Imidazopyrimidines, potent inhibitors of p38 MAP kinase
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The MAP kinase p38 is implicated in the release of the pro-inflammatory cytokines TNF-α and IL-1β. Inhibition of cytokine release may be a useful treatment for inflammatory conditions such as rheumatoid arthritis and Crohn's disease. A novel series of imidazopyrimidines have been discovered that potently inhibit p38 and suppress the production of TNF-α in vivo.
- Rupert, Kenneth C.,Henry, James R.,Dodd, John H.,Wadsworth, Scott A.,Cavender, Druie E.,Olini, Gilbert C.,Fahmy, Bohumila,Siekierka, John J.
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p. 347 - 350
(2007/10/03)
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- Substituted 2-aryl-3-(heteroaryl)-imidazo[1,2-a]pyrimidines, and related pharmaceutical compositions and methods
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This invention relates to a series of imidazopyrimidines of Formula I, and pharmaceutical compositions containing them. The compounds of the invention inhibit the production of a number of inflammatory cytokines and are useful in the treatment and prevention of diseases associated with the overproduction thereof.
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- Heteroaromatic thioether-boronic acid cross-coupling under neutral reaction conditions.
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[reaction: see text] Pi-deficient heteroaromatic thioethers undergo efficient palladium-catalyzed cross-coupling with boronic acids mediated by copper(I) thiophene-2-carboxylate.
- Liebeskind, Lanny S,Srogl, Jiri
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p. 979 - 981
(2007/10/03)
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- An algorithm-directed two-component library synthesized via solid-phase methodology yielding potent and orally bioavailable p38 MAP kinase inhibitors
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Previously we reported the identification of RPR200765A, a potent orally bioavailable pyridine - imidazole inhibitor of p38 mitogen-activated protein (MAP) kinase which suppressed paw swelling and joint pathology in streptococcal cell wall-induced arthrit
- McKenna, Jeffrey M.,Halley, Frank,Souness, John E.,McLay, Iain M.,Pickett, Stephen D.,Collis, Alan J.,Page, Kenneth,Ahmed, Imtiaz
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p. 2173 - 2184
(2007/10/03)
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- Substituted pyridones having cytokine inhibitory activity
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There are disclosed compounds of formula (I) and pharmaceutically acceptable salts thereof which exhibit utility for the treatment of cytokine mediated diseases such as arthritis.
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- RPR203494 a pyrimidine analogue of the p38 inhibitor RPR200765A with an improved in vitro potency
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Following the discovery of RPR200765, a series of pyrimidine analogues have been prepared as backups. Amongst them, RPR203494 was identified with a better in vitro profile than RPR200765A.
- Collis, Alan J,Foster, Martyn L,Halley, Frank,Maslen, Christopher,McLay, Iain M,Page, Kenneth M,Redford,Souness, John E,Wilsher, Nicola E
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p. 693 - 696
(2007/10/03)
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- Substituted imidazoles having cytokine inhibitory activity
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Compounds represented by formula I: STR1 are disclosed. AR represents an aromatic group containing 6-10 atoms; and STR2 represents a 4 to 10 membered non-aromatic heterocycle containing at least one N atom, and optionally containing 1-2 additio
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- Synthesis, antiviral (HSV-1) and antimycotic activities of ethyl or methyl 2,4-disubstituted 5-pyrimidinecarboxylates, 2,4-disubstituted 5-pyrimidinecarboxylic acids and 2,4-disubstituted pyrimidines
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The synthesis of ethyl or methyl 4-substituted or unsubstituted 2-methylthio-5-pyrimidinecarboxylates 3 a-i and 8 o mainly by reaction of ethyl or methyl 2-dimethylaminomethylene-3-oxoalkanoates with 2-methylisothiourea is described. Also some ethyl 2-sub
- Sansebastiano,Mosti,Menozzi,Schenone,Muratore,Petta,Debbia,Pesce Schito,Schito
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p. 335 - 355
(2007/10/02)
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- Synthesis and anxiolytic activity of N-substituted cyclic imides (1R*,2S*3R*,4S*)-N-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-2,3-b icyclo[2.2.1]heptanedicarboxime (Tandospirone) and related compounds
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A series of cyclic imides bearing a ω-(4-aryl and 4-heteroaryl-1-piperazinyl)alkyl moieties was synthesized and tested in vivo for anxiolytic activity. The in vitro binding affinities of these compounds were also examined for 5-HT(1A) receptor sites. Structure-activity relationships within these series are discussed. One of these compounds, (1R*,2S*,3R*,4S*)-N-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-2,3- bicyclo[2.2.1]heptanedicarboximide (1: tandospirone), was found to be equipotent with buspirone in its anxiolytic activity and more anxio-selective than buspirone and diazepam. Tandospirone (1) is currently undergoing clinical evaluation as a selective anxiolytic agent.
- Ishizumi,Kojima,Antoku
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p. 2288 - 2300
(2007/10/02)
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- Highly Regioselective Bromination Reactions of Polymethylpyrimidines
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4,5-Dimethyl- and 4,5,6-trimethyl-substituted pyrimidines are brominated at C5-Me with NBS in CCl4 and at C4(6)-Me with bromine in acetic acid to give the corresponding bromomethyl derivatives in a high yield.The remaining methyl group(s) can also be brominated with high regioselectivity.The 2-methylthio substituent is not oxidized under these conditions.
- Strekowski, Lucjan,Wydra, Roman L.,Janda, Lubomir,Harden, Donald B.
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p. 5610 - 5614
(2007/10/02)
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