摘要:
La présent invention a pour objet des composés répondant à la formule (I) : dans laquelle : - Z représente un groupe N(R 1 )XR 2 , N(R 1 )COOR’ 2 ou OCON(R 1 )R’ 2 ; - X représente un groupe -CO-, -SO 2 -, -CON(R 10 )- ou -CSN(R 10 )- ; - R 1 représente un atome d'hydrogène ou un groupe (C 1 -C 4 )alkyle ; - R 2 représente : . un groupe (C3-C 10 )alkyle ; . un radical carbocyclique non aromatique en (C 3 -C 12 ) ; . un radical hétérocyclique ; . un phényle non substitué ou substitué ; . un (C 1 -C 2 )alkylène substitué par un ou deux substituants identiques ou différents ; - R' 2 représente un phényle non substitué ou substitué ; - R 3 représente un atome d'hydrogène ou un groupe (C 1 -C 4 )alkyle, cyano, (C 1 -C 4 ) alcoxyméthyle ou hydroxyméthyle. Procédé de préparation et application en thérapeutique.
摘要:
The invention relates to N-sulfonyl-alpha-amino-acetic acid derivatives of the general formula (I): including the optical isomers thereof and mixtures of such isomers, wherein Ar1 and Ar2 independently of each other stand for an optionally substituted aryl or heteroaryl group, R1 and R2 stand independently of each other for hydrogen, optionally substituted C1-C5alkyl, optionally substituted C2-C5alkenyl, C-2C5alkynyl or optionally substituted C3C6Cycloalkyl; R3 designates hydrogen, C-3C5alkenyl, C3-C5 alkynyl or optionally substituted C-1C5alkyl; R4 is optionally substituted C1-C5alkyl, optionally substituted C-2C5alkenyl, C-2C5alkynyl or optionally substituted C-3C6 cycloalkyl; R5 and R6 are independently of each other hydrogen or optionally substituted C1-C5alkyl, optionally substituted C2-C5alkenyl, C-2C5alkynyl or optionally substituted C3-C6cycloalkyl; R7 and R8 are independently of each other hydrogen or optionally substituted C1-C5alkyl, optionally substituted C2-C5alkenyl, C2-C5alkynyl or optionally substituted C3-C6cycloalkyl; W designates a bridge selected from -O-, -S-, -SO-, -SO2- or is an -NH- or -N(C1-C5alkyl)- bridge; X designates a direct bond or a bridge selected from -O-, -S-, -SO-, -SO2- or is an -NHor -N(C1C5alkyl)- bridge; Y designates -OR9 or NR10R11; a and b independently of each other stand for a number 1, 2 or 3; and c stands for a number zero, 1 or 2; with R9,R10 and R11 being defined according to the claims. These compounds possess useful plant protecting properties and may advantageously be employed in agricultural practice for controlling or preventing the infestation of plants by phytopathogenic microorganisms, especially fungi.
摘要:
A method is described for the preparation of pyridyl-aryl-sulphonic compounds of formula (I), by cross-coupling reaction, promoted by catalytic systems based on palladium or nickel between compounds of formulae (II, III), in which; a) Met represents Mg or Zn, b) Y represents C1, Br, I or acetoxy, c) Z represents I, Br, Cl, triflate, sulphonate and/or sulphone, d) R 1 , R 2 , R 4 , R 5 , which are the same as one another or different, represent H, a linear and/or branched C 1 -C 4 alkyl, and/or an aryl, and/or a heteroaryl, or R 1 and R 2 and/or R 4 and R 5 , taken together, form a heteroaryl, and e) R 3 represents a linear, branched or cyclic C 1 -C 8 alkyl and/or an aryl, and/or a heteroaryl.
摘要:
A procatalyst complex for the polymerisation of olefins comprising a group III element or a group 3 to 8 transition metal n-bonded by an open n -ligand at least two heteroatoms in the five atom n chain and having an unsaturated ring fused to the first and second atoms of the n chain and a further unsaturated ring fused to the fourth and fifth atoms of the n chain, i.e. (IV) where (a) is an optionally substituted 5 to 12 membered ring; each X independently is C, N, P, B or Si, at least two X's being heteroatoms; a is 0 or 1; R is a C1-16 hydrocarbyl, a tri C1-8 hydrocarbylsilyl or a tri C1-8 hydrocarbylsiloxy group or a group R R where R is a 1 to 4 atom bridge and R is a group capable of o-bonding or n-bonding a transition metal; q is 1, 2 or 3; M is a group III element or a group 3 to 8 transition metal; L is a n-ligand; r is zero, 1 or 2; Z is a o-ligand; and s is zero or a positive integer having a value of up to 3.
摘要翻译:用于烯烃聚合的前催化剂络合物,其包含III族元素或3至8族过渡金属,其通过在5个原子n5链中具有至少两个杂原子并且具有不饱和键 环与n 5链的第一和第二个原子融合,另一个不饱和环与n 5链的第四和第五个原子稠合,即(IV),其中(a)是任选取代的5至12个 元环 每个X独立地是C,N,P,B或Si,至少两个X是杂原子; a是0或1; R是C1-16烃基,三C1-8烃基甲硅烷基或三C1-8烃基甲硅烷氧基或基团R a R b,其中R a是1至4个原子桥,R b, 是能够使过渡金属O键合或n键合的基团; q为1,2或3; M是III族元素或3至8族过渡金属; L是n-配体; r为零,1或2; Z是O-配体; 并且s为零或具有高达3的值的正整数。
摘要:
The present invention relates to novel 2-aminopyridine derivative compounds of formula (I) wherein R to R have the meanings provided herein. The invention further relates to combinatorial libraries containing two or more such compounds, as well as methods of preparing 2-aminopyridine derivative compounds.
摘要:
Compounds of Formula (1), Formula (2), Formula (3) and Formula (4) wherein the symbols have the meaning assigned to them in the disclosure have retinoid-like biological activity.
摘要:
The present invention is directed to pyrrolidine compounds of formula (I) (wherein R , R , R , R , R , R , R and n are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-5 and/or CCR-3.
摘要:
Novel GRP receptor antagonists are provided. Methods of using the present compounds to antagonize GRP receptors are also provided. The present invention further involves the synthesis of the present compounds.
摘要:
Acyl guanidines are provided which are sodium/proton exchange (NHE) inhibitors which have structure (I) wherein n is 1 to 5; X is N or C-R wherein R is H, halo, alkenyl, alkynyl, alkoxy, alkyl, aryl or heteroaryl; and R , R , R and R are as defined herein, and where X is N, R is preferably aryl or heteroaryl, and are useful as antianginal and cardioprotective agents. In addition, a method is provided for preventing or treating angina pectoris, cardiac dysfunction, myocardial necrosis, and arrhythmia employing the above acyl guanidines.
摘要:
The present invention relates to inhibitors of p38, a mammalian protein kinase involved in cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.