摘要:
The invention provides compounds of the formula (I) wherein the variables are as defined in the specification.The compounds of the invention are inhibitors of metalloproteinase MMP-12 and are among other things useful for the treatment of obstructive airway diseases, such as chronic obstructive pulmonary disease (COPD).
摘要:
A compound of the formula II wherein one of R1 and R2 is halo and the other is H or halo; R3 is C1-C4 straight or branched chain, optionally fluorinated, alkyl; R4 is H; or R3 together with R4 and the adjoining backbone carbon defines: a spiro-C5-C7 cycloalkyl, optionally substituted with 1 to 3 substituents selected from halo, hydroxyl, C1-C4 alkyl or C1-C4 haloalkyl; or optionally bridged with a methylene group; or a C4-C6 saturated heterocycle having a hetero atom selected from O, NRa, S, S(═O)2; where Ra is H, C1-C4 alkyl or CH3C(═O); R5 is independently selected from H or methyl; E is —C(═O)—, —S(═O)m—, —NR5S(═O)m—, —NR5C(═O)—, —OC(═O)—, R6 is a stable, optionally substituted, monocyclic or bicyclic, carbocycle or hetorocycle; m is independently 0, 1 or 2; are inhibitors of cathepsin K and useful in the treatment or prophylaxis of osteoporosis.
摘要:
The present invention relates to the field of compounds which are substrates or inhibitors of proteolytic enzymes and to apparatus and methods for identifying substrates or inhibitors for proteolytic enzymes. We have devised a combinatorial method for the rapid indentification of binding motifs which will greatly expedite the synthesis of inhibitors of a variety of proteolytic enzymes such as aspartyl proteases, serine proteases, metallo proteases and cysteinyl proteases.
摘要:
The present invention provides a method of producing improved infant care articles characterized by the inclusion of a non-toxic, non-irritating phosphorescent material with the material of construction of components of the infant care articles so that such components phosphorescently emit light visible in a darkened environment, allowing the location and position of the articles to be readily determined without the need for an additional light source. Embodiments of infant care articles produced in accordance with the invention, including infant pacifiers, bottle assemblies, and clothing, are disclosed.
摘要:
The invention provides novel compounds of formula I having the general formula: wherein R1, R2, R3, X and Y are as described herein. Accordingly, the compounds may be provided in pharmaceutically acceptable compositions and used for the treatment of immunological or hyperproliferative disorders.
摘要:
The present invention provides a novel class of pyridyl-amine fused azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators.
摘要:
A compound of the formula II wherein one of R1 and R2 is halo and the other is H or halo; R3 is C1-C4 straight or branched chain, optionally fluorinated, alkyl; R4 is H; or R3 together with R4 and the adjoining backbone carbon defines: a spiro-C5-C7 cycloalkyl, optionally substituted with 1 to 3 substituents selected from halo, hydroxyl, C1-C4 alkyl or C1-C4 haloalkyl; or optionally bridged with a methylene group; or a C4-C6 saturated heterocycle having a hetero atom selected from O, NRa, S, S(═O)2; where Ra is H, C1-C4 alkyl or CH3C(═O); R5 is independently selected from H or methyl; E is —C(═O)—, —S(═O)m—, —NR5S(═O)m—, —NR5C(═O)—, —OC(═O)—, R6 is a stable, optionally substituted, monocyclic or bicyclic, carbocycle or heterocycle; m is independently 0,1 or 2; are inhibitors of cathepsin K and useful in the treatment or prophylaxis of osteoporosis.
摘要:
An environmentally friendly vegetation growth-enhancing erosion control blanket is formed from an elongated rectangular excelsior/wood wool mat. The mat is held together with threads stitched therein. When the finished blanket is placed atop the ground, the blanket serves to shield the earth area from wind and water erosion forces, without the presence of the plastic netting often used in the prior art. As the ground vegetation grows, it ultimately replaces the blanket which decomposes and furnishes the ground vegetation with a nutritive mulch.
摘要:
A system and methods for using data from an external database compiled from real device used for testing and simulation of a system. The system includes an external database interface to access an external database. The external database includes a plurality of categories of time-value data collected from an electrical device. An importer converts one of plurality of categories of time-value data to a corresponding topic of a common data format. A device profiler is coupled to the importer to create a device profile including the converted topic. A database profiler creates a database profile representing a system including a device defined by the device profile and including the category of time-value data.
摘要:
The invention provides compounds of the formula (I) wherein the variables are as defined in the specification. The compounds of the invention are inhibitors of metalloproteinase MMP-12 and are among other things useful for the treatment of obstructive airway diseases, such as chronic obstructive pulmonary disease (COPD).