摘要:
The invention relates to 4-propargyloxy-benzyl dervatives of the general formula (I ) including the optical isomers thereof and mixtures of such isomers, wherein R 1 is hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl or optionally substituted aryl; R 2 , R 3 , R 5 , R 6 , and R 7 are each independently of each other hydrogen or optionally substituted alkyl; R 4 is optionally substituted alkyl; X is O or N-R 7 ; and R 8 is a group R 9 is optionally substituted aryl or optionally substituted heteroaryl; R 10 and R 11 are each independently hydrogen, optionally substituted alkyl, optionally substituted alkenyl or optionally substituted alkynyl; R 12 is optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted aryl or optionally substituted heteroaryl; R 13 is hydrogen or optionally substituted alkyl, alkenyl or alkynyl; and R 14 is optionally substituted alkyl or optionally substituted amino. 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:
Universal supports for oligonucleotide synthesis include a support material represented by the formula (I). In this formula, substituent A is selected from H, alkyl, aryl, or a polymeric or silica base material; substituent B is selected from acyl, aroyl or a polymeric or silica base material; and substituent C is selected from a dimethoxytrityl group or a protecting group removable under acidic or neutral conditions. For the supports, one of substituents A or B constitutes the polymeric or silica base material. In use, an oligonucleotide is attached to the support at substituent C.
摘要:
Compound of formula (I) or therapeutically acceptable salts thereof, are protein tyrosine kinase PTP1B inhibitors. Preparation of the compounds, compositions containing the compounds, and treatment of diseases using the compounds are disclosed.
摘要:
The present invention relates to the inhibition of HIV integrase, and to the treatment of AIDS or ARC by administering compounds of the formula (Ia) wherein R is C1-C4 alkyl, carbocyclic radical, heterocyclic radical, aryl-C1-C2 alkylene, aryloxy-C1-C2 alkylene, alkoxy-CC(O)-, wherein R is optionally substituted from 1-3 times with halo, C1-C2 alkyl or C1-C2 alkoxy, or R is H; R is H or C1-C4 alkyl; R is H, C1-C4 alkyl or phenyl-C0-C2 alkylene which is optionally substituted with 1-3 R ; R is carbocylic radical, heterocyclic radical, aryloxy, aryl-C1-C4 alkylene, aryl-cyclopropylene, aryl-NHC(O)-, wherein R is optionally substituted with 1-3 R ; and wherein each R is independently selected from H, halo, C1-C4 alkyl, C1-C4 alkenyl, C1-C4 haloalkyl, C1-C4 alkoxy, R -phenyl, R -phenoxy, R -benzyl, R -benzyloxy, NH2C(O)-, alkyl-NHC(O)-, wherein R is H, halo; Z is a bond or a substituted or unsubstituted C1-C4 alkylene group; and B is formula (a), (b), or (c).
摘要:
A method for sequentially performing a synthesis, separation and screening of chemical entities, especially a combinatorial library, is described. The method utilises a bulk of a stationary phase (e.g. silica gel, aluminium oxide, cellulose, etc. for example arranged on a backing) for the performance of the synthesis, separation and screening. The technique described enables a rapid route from synthesis to the testing of chemical compounds. Screening can be performed without need for reaction work-up. Preferred screening methods are those used to determine the biological activity of the compounds.
摘要:
The present invention relates to small molecules according to formula (I) which are potent inhibitors of a alpha 4 beta 1 mediated adhesion to either VCAM or CS-1 and which can be used for treating or preventing alpha 4 beta 1 adhesion mediated conditions in a mammal such as a human.
摘要:
The present invention is directed to novel modulators of the NMDA receptor. Separate aspects of the inventions are directed to pharmaceutical compositions comprising said compounds and uses of the compounds to treat neurological disorders or neuropsychiatric disorders such as depression.
摘要:
A personal care composition comprising N-aralkylcarbonyldiamines. When such compounds are used in personal care compositions, they have been unexpectedly shown to enhance cell proliferation and epidermal thickness, traits associated with younger, healthy looking skin.
摘要:
The present invention relates to new classes of monomeric compounds, which may be polymerized to form novel biodegradable and bioresorble polymers and co-polymers. These polymers and co-polymers, while not limited thereto, may be adapted for radio- opacity and are useful for medical device applications and controlled release therapeutic formulations.