Abstract:
The present invention provides a lipid compound comprising at least one non-polar moiety and a polar moiety, wherein each or at least one non-polar moiety is of the formula X—Y-Z-, wherein X is a hydrocarbyl chain, Y is selected from at least one of S, Se, SO2, SO, and O, and Z is an optional hydrocarbyl group, wherein the polar moiety is of the formula —[C(O)]mPHG, wherein PHG is a polar head group, and wherein m is the number of non-polar moieties.
Abstract translation:本发明提供了包含至少一个非极性部分和极性部分的脂质化合物,其中每个或至少一个非极性部分具有式XYZ-,其中X是烃基链,Y至少选自 S,Se,SO 2,SO和O之一,Z是任选的烃基,其中极性部分具有式 - [C(O)] m - PHG,其中PHG是极性头基,并且其中m是非极性部分的数目。
Abstract:
A piston includes a piston body having a longitudinal central axis. A piston head is formed with a plurality of ring grooves and a pair of pin bosses depend from the head and are formed with a pair of pin bores that are centered on a common pin bore axis that intersects the longitudinal axis of the piston. Skirt Portions have outer surfaces with a longitudinal profile that is convexly shaped. A major diameter of the profile lies within ±2 mm of the pin bore axis in both a cold and hot condition.
Abstract:
The present invention provides a process for preparing a modified lipid of the formula comprising reacting (I) a compound of the formula; and (ii) a compound of the formula wherein component (ii) is formulated as a liposome; wherein B is a lipid; wherein A is a moiety of interest (MOI) and is a hydrocarbyl group; wherein X is an optional linker group; wherein R1 is H or a hydrocarbyl group; and wherein R2 is a lone pair, H or a hydrocarbyl group. The moiety of interest A may be selected from a carbohydrate moiety, a polymer, a peptide, a glycoprotein, a small biomolecule (such as a folic acid derivative) and a bioconjugate linker.
Abstract:
Methods for isolating K+Hnov genes are provided. The K+Hnov nucleic acid compositions find use in identifying homologous or related proteins and the DNA sequences encoding such proteins; in producing compositions that modulate the expression or function of the protein; and in studying associated physiological pathways. In addition, modulation of the gene activity in vivo is used for prophylactic and therapeutic purposes, such as identification of cell type based on expression, and the like.
Abstract translation:提供了分离K + Hnov基因的方法。 K + Hnov核酸组合物用于鉴定同源或相关蛋白质和编码此类蛋白质的DNA序列; 在制备调节蛋白质的表达或功能的组合物中; 并研究相关的生理学途径。 此外,体内基因活性的调节用于预防和治疗目的,例如基于表达的细胞类型的鉴定等。
Abstract:
The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
Abstract:
A pharmaceutical or veterinary composition comprising a compound of formula I ##STR1## wherein X is a --CO.sub.2 H group and R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 are as defined in the specification, or a salt, hydrate or solvate thereof, and a pharmaceutically or veterinarily acceptable excipient or carrier. A method of treatment of diseases or conditions mediated by MMPs in mammals, such as rheumatoid arthritis, osteoarthritis, periodontitis, gingivitis, corneal ulceration or tumour invasion by secondary means, by administering to the mammal an effective amount of the composition.
Abstract:
Matrix metalloproteinase inhibiting compounds of formula (I), wherein X is a --CO.sub.2 H or --CONHOH group; and one of the groups proximate to the amide bonds is a steric bulky group, showing enhanced oral absorption. ##STR1##
Abstract:
Compounds of general formula (I), principally characterized in that R4 is a polyether group, are water soluble matrix metalloproteinase inhibitors. ##STR1##
Abstract:
Compounds of general formula (I), wherein W represents a 5- or 6-membered aromatic heterocyclic ring containing one or more non-quaternised sp2 nitrogen atoms in its ring, which heterocyclic ring may be optionally fused to a benzene ring or to a further 5- or 6-membered aromatic heterocyclic ring containing one or more nitrogen atoms, wherein at least one of the said heterocyclic rings may also contain an oxygen or sulphur atom, and wherein any of the rings may be optionally substituted with one or more substituents selected from --C.sub.1 -C.sub.6 alkyl, --OC.sub.1 -C.sub.6 alkyl, halo, --CF.sub.3 and --CN; Z represents a) a divalent alkanediyl group from 1 to 8 carbon atoms which may be a straight or branched-chain, wherein the said group is either unsubstituted or substituted by one or more substituents selected from hydroxy, --OC.sub.1 -C.sub.6 alkyl, --SC.sub.1 -C.sub.6 alkyl and halo; or b) a divalent alkenediyl or alkynediyl group from 2 to 8 carbon atoms which may be a straight or branched-chain, wherein the said group is either unsubstituted or subtituted by one or more substituents selected from hydroxy, --OC.sub.1 -C.sub.6 alkyl, --SC.sub.1 -C.sub.6 alkyl and halo; R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, and R.sup.6 each represents a hydrogen atom, a --C.sub.1 -C.sub.18 alkyl or a --C.sub.2 -C.sub.18 alkenyl group; or R.sup.3 and R.sup.5 together with the carbon atoms to which they are attached can form a five to ten membered monocycycloalkyl or bicycloalkyl ring which may be optionally substituted with one or more substituents selected from --C.sub.1 -C.sub.6 alkyl, --OC.sub.1 -C.sub.6 alkyl, halo, --CF.sub.3 and --CN; or R.sup.3, R.sup.4 and R.sup.5, R.sup.6 and the carbon atoms to which they are attached form a phenyl ring which may be optionally substituted with one or more substituents selected from --C.sub.1 -C.sub.6 alkyl, --OC.sub.1 -C.sub.6 alkyl, halo, --CF.sub.3 and --CN; X represents a bond, an oxygen atom, a sulphur atom, a --NH-- group, a --N(C.sub.1 -C.sub.6 alkyl)-- group, a --(CH.sub.2).sub.n -- group or a --CR.sup.7 R.sup.8 -- group; n represents an integer of 1, 2 or 3; R.sup.7 and R.sup.8 each represents a --C.sub.1 -C.sub.18 alkyl or a --C.sub.2 -C.sub.18 alkenyl group; or R.sup.3 and R.sup.7 together with the carbon atoms to which they are attached can form a five to ten membered monocycloalkyl or bicycloalkyl ring which may be optionally substituted with one or more substituents selected from --C.sub.1 -C.sub.6 alkyl, --OC.sub.1 -C.sub.6 alkyl, halo, --CF.sub.3 and --CN; or R.sup.3, R.sup.4 and R.sup.7, R.sup.8 and the carbon atoms to which they are attached form a phenyl ring which may be optionally substituted with one or more substituents selected from --C.sub.1 -C.sub.6 alkyl, --OC.sub.1 -C.sub.6 alkyl, halo, --CF.sub.3 and --CN; and their pharmaceutically and veterinarily acceptable acid addition salts and hydrates are antagonists of platelet activating factor (PAF) and as such are useful in the treatment or amelioration of various diseases or conditions mediated by PAF.