摘要:
The present invention provides a compound having aggrecanase inhibitory activity and MMP-13 inhibitory activity, and useful as a therapeutic agent for osteoarthritis, rheumatoid arthritis and the like, more specifically, a cyclopropane compound of formula (1): wherein R1 is —(CH2)m—X—(CH2)n-A1 etc., wherein m and n are the same or different and each is 0 to 6, X1 is a single bond, etc. and A1 is a substituted C3-14 hydrocarbon ring group, etc.; R2 and R3 are the same or different and each is a hydrogen atom, —(CH2)p—X1-(CH2)q-A2, etc., wherein p and q are the same or different and each is 0 to 6, X1 is a single bond, etc. and A2 is an optionally substituted C3-14 hydrocarbon ring group, etc.; R4 is —CO2R9, etc., wherein R9 is a hydrogen atom, etc.; and R20 and R21 are the same or different and each is a hydrogen atom, —(CH2)m12—X12—(CH2)m12—R30, etc., wherein m12 and m12 are the same or different and each is 0 to 6, X12 is a single bond, etc. and R30 is a hydrogen atom, etc.; or a prodrug thereof or a pharmaceutically acceptable salt thereof.
摘要:
The present invention provides a compound having aggrecanase inhibitory activity and MMP-13 inhibitory activity, and useful as a therapeutic agent for osteoarthritis, rheumatoid arthritis and the like, more specifically, a N-substituted-N-sulfonylaminocyclopropane compound of formula (1): wherein R1 is —W-A1—W1-A2, W is —(CH2)m—X—(CH2)n—, wherein W1 is —(CH2)m1—X1—(CH2)n1—, m, m1, n and n1 are the same or different and each is 0 to 6, X and X1 are the same or different and each is a single bond, etc., A1 is an optionally substituted C3-14 hydrocarbon ring group, etc. and A2 is a substituted C3-14 hydrocarbon ring group etc.; R2 is —(CH2)r—CO—R8, etc., wherein r is 0 to 6 and R8 is a C1-6 alkoxy group, etc.; R3 and R4 are the same or different and each is a hydrogen atom, a C1-6 alkyl group, etc.; and R5 is —CO2R21 etc.; R30 and R31 are the same or different and each is a hydrogen atom, etc.; or a prodrug thereof or a pharmaceutically acceptable salt thereof.
摘要:
This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders.
摘要:
A calibration standard which may be used to calibrate lateral dimensional measurement systems is provided. The calibration standard may include a first substrate spaced from a second substrate. In addition, the calibration standard may include at least one layer disposed between the first and second substrates. The layer may have a traceably measured thickness. For example, a thickness of the layer may be traceably measured using any measurement technique in which a measurement system may be calibrated with a standard reference material traceable to a national testing authority. The calibration standard may be cross-sectioned in a direction substantially perpendicular to an upper surface of the first substrate. The cross-sectioned portion of the calibration standard may form a viewing surface of the calibration standard. In this manner, a lateral dimensional artifact of the calibration standard may include the traceably measured thickness of at least the one layer.
摘要:
Compounds of Formula I: (Formula should be inserted here) and stereoisomers and pharmaceutically acceptable salts and solvates thereof in which R1, R2, R3, R4, R5, R6, R7, X1 and X2 have the meanings given in the specification, are inhibitors of one or more JAK kinases and are useful in the treatment of autoimmune diseases, inflammatory diseases, rejection of transplanted organs, tissues and cells, as well as hematologic disorders and malignancies and their co-morbidities.
摘要:
This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders.
摘要:
This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders.
摘要:
A calibration standard, for calibrating lateral or angular dimensional measurement systems, is provided. The standard may include a first substrate spaced from a second substrate. The standard may be cross-sectioned in a direction substantially perpendicular or substantially non-perpendicular to an upper surface of the first substrate. The cross-sectioned portion of the standard may form a viewing surface of the calibration standard. The standard may include at least one layer disposed between the first and second substrates. The layer, or a feature etched into the first or second substrate or a feature etched into the layer may have a traceably measured thickness or may be oriented at a traceably measured angle with respect to the viewing surface. A thickness or angle of the layer or other feature may be traceably measured using any technique for calibrating a measurement system with a standard reference material traceable to a national testing authority.
摘要:
Compounds of Formula I are useful for inhibition of Raf kinases. Methods of using compounds of Formula I and stereoisomers, tautomers and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed. [FORMULA I]
摘要:
The compound of Formula (I) and pharmaceutically acceptable salts and prodrugs thereof are useful in the treatment and prevention of various disorders mediated by kinases.