cas 17119-73-2, 4-Chloro-6-methyl-2-(methylthio)pyrimidine

Articles about 17119-73-2Total 17 be found

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Some Features of the Reaction of 6-Methyl-2S-substituted Pyrimidin-4-ols with the Vilsmeier–Haack Reagent
Abstract: Formylation of 6-methyl-2S-substituted pyrimidin-4-ols under the conditions of the Vilsmeier–Haack reaction leads to the formation of nucleophilic substitution products of the hydroxyl group. The formation of the expected formylation products does not occur.
Ofitserova, E. S.,Shklyarenko, A. A.,Yakovlev, I. P.
p. 750 - 752
(2020)
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Synthesis and preliminary biological properties assessment of novel 2-s-, 4-, 5-substituted and bicyclic derivatives of 6-methylpyrimidine-4-ol
A series of novel 2-S-, 4-, 5-substituted and bicyclic 6-methylpyrimidine-4-ol derivatives including pyrazole, 1,2,4-triazole and pyridazine moieties in the molecule were synthesized by accessible and efficient methods. Thiopyrazolyl derivatives were obta
Ayvazyan, Armen G.,Azaryan, Zhermen A.,Ghazaryan, Emma A.,Pivazyan, Vergush A.,Tamazyan, Rafael A.,Yengoyan, Aleksandr P.
p. 149 - 156
(2020/02/04)

Substituted 5-Hetaryl-4-Aminopyrimidines
The present invention relates to the use of 5-hetaryl-4-aminopyrimidines of the formula I and their salts for controlling plant-damaging fungi. The invention also relates to novel 5-hetaryl-4-aminopyrimidines and to crop protection compositions comprising at least one such compound as active component. Het is an optionally substituted 5- or 6-membered aromatic heterocycle which has 1, 2, 3 or 4 heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur as ring members, where the 5- or 6-membered heteroaromatic radical may have 1, 2, 3 or 4 identical or different substituents L, R1, R2 are inter alia hydrogen, C1-C8-alkyl, C3-C8-cycloalkyl, C5-C10-bicycloalkyl, C2-C8-alkenyl, C4-C10-alkadienyl, C3-C6-cycloalkenyl, C2-C8-alkynyl, phenyl, naphthyl or a five- or six-membered saturated, partially unsaturated or aromatic heterocycle which has one, two, three or four heteroatoms from the group consisting of O, N or S as ring members; or together form a ring; R3 is inter alia hydrogen, OH, halogen, cyano, NR31R32, C1-C8-alkyl, C1-C8-alkoxy, C1-C8-alkylthio, C1-C8-alkylsulfinyl, C1-C8-alkylsulfonyl, C2-C8-alkenyl or C2-C8-alkynyl, and R4 is halogen, cyano, hydroxyl, mercapto, N3, C1-C6-alkyl, C2-C8-alkenyl, C2-C8-alkynyl, C1-C6-haloalkyl, C1-C6-alkoxy, C3-C8-alkenyloxy, C3-C8-alkynyloxy, C1-C6-haloalkoxy, C1-C6-alkylthio, C3-C8-alkenylthio, C3-C8-alkinylthio, C1-C6-haloalkylthio, or is a radical of the formula C(═Z)OR41, C(═Z)NR42R43, C(═Z)NR44—NR42R43, C(═Z)R45, CR46R47—OR48, CR46R47—NR42R43, ON(═CR49R50), O—C(═Z)R45, NR42R43a, NR51(C(═Z)R45), NR51(C(═Z)OR41), NR51(C(═Z)—NR42R43), NR52a(N═CR49R50), NR52NR42R43, NR52OR41 or C(═N—X—R45)SR41.
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Page/Page column 36-37

(2011/09/14)

1-(Pyrimidin-4-yl)pyrazol-5(4H)-one derivatives: I. Synthesis of 3-methyl-1-(6-methyl-2-methylsulfanylpyrimidin-4-yl)-pyrazol-5-ol and specificity of its Knoevenagel reaction
3-Methyl-1-(6-methyl-2-methylsulfanylpyrimidin-4-yl)-1H-pyrazol-5-ol available via cyclocondensation of 6-methyl-2-methylsulfanylpyrimidin-4- ylhydrazine with ethyl acetoacetate reacted with aromatic aldehydes to give two kinds of products, 4-arylmethylid
Erkin,Krutikov
experimental part
p. 392 - 396
(2011/06/27)

Arylpiperazine-containing pyrimidine 4-carboxamide derivatives targeting serotonin 5-HT2A, 5-HT2C, and the serotonin transporter as a potential antidepressant
Pyrimidine usually has good pharmacokinetic properties as a drug substance and considerable efforts have been devoted to develop pyrimidine derivatives into drug candidates. Arylpiperazine-containing pyrimidine 4-carboxamide derivatives were synthesized and evaluated for binding to serotonin receptors and transporter. Pyrimidine derivatives showed good antidepressant activity in FST (forced swimming test) animal model and also displayed no appreciable inhibitory activity against hERG channel blocking assay. Herein SAR studies of pyrimidine derivatives targeting serotonin receptors and transporter will be disclosed.
Kim, Jong Yup,Kim, Deukjoon,Kang, Suk Youn,Park, Woo-Kyu,Kim, Hyun Jung,Jung, Myung Eun,Son, Eun-Jung,Pae, Ae Nim,Kim, Jeongmin,Lee, Jinhwa
scheme or table
p. 6439 - 6442
(2010/11/18)

METHODS OF TREATING CANCER USING PYRIDOPYRIMIDINONE INHIBITORS OF PI3K ALPHA
The present invention provides methods of treating cancer by administering a compound of Formula I, optionally as a pharmaceutically acceptable salt, solvate and/or hydrate thereof, in combination with other cancer treatments. (Formula I)
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Page/Page column 259

(2008/12/04)

PYRIDO [2, 3-D] PYRIMIDIN-7-ONE COMPOUNDS AS INHIBITORS OF PI3K-ALPHA FOR THE TREATMENT OF CANCER
The invention is directed to a Compound of Formula I, II, or III. The invention provides compounds that inhibit, regulate, and/or modulate PI3K that are useful in the treatment of hyperproliferatives diseases, such as cancer.
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Page/Page column 70; 78-79

(2008/12/08)

Design, synthesis, and activity of 2-imidazol-1-ylpyrimidine derived inducible nitric oxide synthase dimerization inhibitors
By the screening of a combinatorial library for inhibitors of nitric oxide (NO) formation by the inducible isoform of nitric oxide synthase (iNOS) using a whole-cell assay, 2-(imidazol-1-yl)pyrimidines were identified. Compounds were found to inhibit the dimerization of iNOS monomers, thus preventing the formation of the dimeric, active form of the enzyme. Optimization led to the selection of the potent, selective, and orally available iNOS dimerization inhibitor, 21b, which significantly ameliorated adjuvant-induced arthritis in a rat model. Analysis of the crystal structure of the 21b-iNOS monomer complex provided a rationalization for both the SAR and the mechanism by which 21b blocks the formation of the protein-protein interaction present in the dimeric form of iNOS.
Davey, David D.,Adler, Marc,Arnaiz, Damian,Eagen, Keith,Erickson, Shawn,Guilford, William,Kenrick, Margaret,Morrissey, Michael M.,Ohlmeyer, Mike,Pan, Gonghua,Paradkar, Vidyadhar M.,Parkinson, John,Polokoff, Mark,Saionz, Kurt,Santos, Cecile,Subramanyam, Babu,Vergona, Ron,Wei, Robert G.,Whitlow, Marc,Ye, Bin,Zhao, Zuchun,Devlin, James J.,Phillips, Gary
p. 1146 - 1157
(2007/10/03)

NOVEL SUBSTITUTED IMIDAZOLE DERIVATIVES
The present invention relates to a compound represented by Formula [I] or a pharmaceutically acceptable salt or ester thereof: wherein: X1, X2, X3, and X4, which may be identical or different, are each C or N, provided that none to two of X1, X2, X3, and X4 is/are N; Y is CH or N; R1, R1', R2, R2', R3, R3', R4, and R4', which may be identical or different, are each a hydrogen atom, a lower alkyl group, or the like; R5 is a hydrogen atom or a methyl group; R6 and R7, which may be identical or different, are each a hydrogen atom, a lower alkyl group, or the like; R8 and R8', which may be identical or different, are each a hydrogen atom, a lower alkyl group, or the like; R9 is an aryl group or a heteroaryl group which may be substituted; and n is an integer from 1 to 3, and a PLK1 inhibitor or an anticancer agent containing the same.
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Page/Page column 56

(2010/11/27)

PYRIDOPYRIMIDINONE INHIBITORS OF PI3Kα
The invention is directed to Compounds of Formula I and pharmaceutically acceptable salts or solvates thereof, as well as methods of making and using the compounds.
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Page/Page column 62

(2008/06/13)

SELECTIVE INHIBITORS AGAINST Cdk4 AND Cdk6 HAVING AMINOTHIAZOLE SKELETON
The present invention relates to a compound represented by Formula [I]: wherein X is O, S, NH or CH 2 ; Y 1 , Y 2 , Y 3 , Y 4 and Y 5 , which may be identical or different, are each CH or N; however, at least one of Y 1 , Y 2 , Y 3 , Y 4 and Y 5 is N; Z 1 and Z 2 , which may be identical or different, are each CH or N; n is an integer from 1 to 3; R 1 is a C 3 -C 8 cycloalkyl group, a C 6 -C 10 aryl group, an aliphatic heterocyclic ring or an aromatic heterocyclic ring, or a bicyclic aliphatic saturated hydrocarbon group; R 2 and R 3 , which may be identical or different, are each a hydrogen atom, a lower alkyl group, a lower alkenyl group, a C 3 -C 8 cycloalkyl group, a C 6 -C 10 aryl group, an aromatic heterocyclic ring, or the like; and R 4 is a hydrogen atom, a lower alkyl group, a C 3 -C 6 cycloalkyl group or the like, or a pharmaceutically acceptable salt or ester thereof, and a selective inhibitor against Cdk4 and/or Cdk6 or an anticancer agent containing the compound or a pharmaceutically acceptable salt or ester thereof.
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Page/Page column 34

(2010/11/25)

ARYL PYRIMIDINE DERIVATIVES
The disclosed pyrimidine derivatives, and pharmaceutically acceptable salts and N-oxides thereof, exhibit useful pharmacological properties, in particular use as selective 5HT2B-antagonists. The invention is also directed to formulations and methods for t
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Page/Page column 26

(2010/10/20)

Bradykin B1receptor antagonists
Bradykinin B1-receptor antagonists of formula are disclosed. The compounds are useful for treating diseases associated with inappropriate bradykinin receptor activity, such as diabetic vasculopathy, inflammation, pain, hyperalgesia, asthma, rhinitis, septic shock, atherosclerosis and multiple sclerosis. Pyrimidines, triazines, and anilines in which Q is imidazolyl or pyrrolyl are particularly preferred.
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Page 22; 23

(2010/02/05)

ARYL PYRIMIDINE DERIVATIVES
The disclosed pyrimidine derivatives, and pharmaceutically acceptable salts and N-oxides thereof, exhibit useful pharmacological properties, in particular use as selective 5HT 2B-antagonists. The invention is also directed to formulations and methods for treatment.
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(2008/06/13)

ARYL PYRIMIDINE DERIVATIVES AND USES THEREOF
The aryl pyrimidine derivatives and pharmaceutically acceptable salts and N-oxides thereof, exhibit useful pharmacological properties, including utility as selective 5HT 2B-antagonists. The 5-HT 2B antagonist is a compound of the formula: STR1 wherein: R. sup.1 is hydrogen, alkyl, lower alkoxy, hydroxyalkyl, cycloalkyl, cycloalkyl lower alkyl, alkenyl, lower thioalkoxy, halo, fluoroalkyl,--NR 6 R. sup.7,--CO 2 R 8,--O(CH 2) n R 9, or lower alkyl optionally substituted with hydroxy, alkoxy, halo, or aryl; in which n is 1, 2, or 3;R 6 and R 7 are hydrogen or lower alkyl; R 8 is hydrogen or lower alkyl; andR 9 is hydrogen, lower alkyl, hydroxy, hydroxy lower alkyl, lower alkenyl, or lower alkoxy;R. sup.2 is hydrogen, lower alkyl, lower alkoxy, halo, or lower fluoroalkyl; R 3 is optionally substituted aryl other than pyridyl, thienyl, or furanyl;R 4 is hydrogen, lower alkyl, cycloalkyl, alkenyl, acyl, amino, amido, aryl,--(CH 2) m NR. sup.10 R 11, or lower alkyl optionally substituted by amino, monosubstituted amino, disubstituted amino, hydroxy, carboxy, aryl, lower alkoxy, amido, alkoxy carbonyl, tetrahydrofuran-2-yl, hydroxyalkoxy, or sulfonamido;in whichR 10 and R. sup.11 are hydrogen or lower alkyl; andR 5 is hydrogen or lower alkyl; provided that: (i) when R 3 is naphthyl, indol-1-yl, or 2,3-dihydroindol-1-yl, and R 2, R 4 and R 5 are all hydrogen, R. sup.1 is not methyl; (ii) when R 3 is phenyl or naphthyl, R 1 is not--NR 6 R 7 ;(iii) when R 3 is phenyl, R 2 is not lower alkoxy, and R 1 and R 2 are not halo;(iv) when R 3 is phenyl and R 1 is H, R 2 is not methyl; and (v) when R 3 is 1,2,3,4-tetrahydroquinolinyl, R 4 and R. sup.5 are hydrogen;or a pharmaceutically acceptable salt or N-oxide thereof.
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(2008/06/13)

ARYL PYRIMIDINE DERIVATIVES
The aryl pyrimidine derivatives and pharmaceutically acceptable salts and N-oxides thereof, exhibit useful pharmacological properties, including utility as selective 5HT 2B-antagonists.
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(2008/06/13)

Angiotensin II receptor antagonists
Compounds are disclosed having the formula: STR1 The compounds of the invention are angiotensin II receptor antagonists.
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(2008/06/13)