摘要:
A compound or pharmaceutically acceptable salts thereof of Formula (I) wherein the substituents are as defined herein, which are useful as kinase inhibitors.
摘要:
Novel compounds of Formula (I) or pharmaceutically acceptable salts, prodrugs and biologically active metabolites thereof of Formula (I) wherein the substituents are as defined herein, which are useful as therapeutic agents.
摘要:
An catalytic converter is integrated with a flexible endcone to form an assembly. The assembly comprises a catalytic converter with a flexible endcone integrated connected to one end of the catalytic converter, which is optionally attached to a mounting flange or exhaust pipe. The endcone comprises a flexible bellow containing a plurality of undulating ribs. The flexible bellow is secured to an end of the catalytic converter at one or more interface points along the periphery of the flexible endcone assembly.
摘要:
The present invention provides paclitaxel derivatives of formula I ##STR1## in which R.sup.1 is --COR.sup.z, in which R.sup.z is RR.sup.o N--, RHN--, RO-- or R;R.sup.2 is C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-6 cycloalkyl, or a radical of the formula --W--R.sup.x in which W is a bond, C.sub.2-6 alkenediyl, or --(CH.sub.2).sub.t --, in which t is one to six; and R.sup.x is naphthyl, phenyl, or heteroaryl, and furthermore R.sup.x can be optionally substituted with one to three same or different C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halogen or --CF.sub.3 groups;R and R.sup.o are independently C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.3-6 cycloalkyl, C.sub.2-6 alkynyl, or phenyl, optionally substituted with one to three same or different C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halogen or --CF.sub.3 groups.Also provided by this invention are pharmaceutical formulations (compositions) and a method of treating mammalian tumors with a compound of formula I.
摘要:
Disclosed are ketone substituted benzimidazole compounds of formula(I): wherein R1, R2, R3, R4 and Xa are defined herein. The compounds of the invention inhibit Itk kinase and are therefore useful for treating diseases and pathological conditions involving inflammation, immunological disorders and allergic disorders. Also disclosed are processes for preparing these compounds and to pharmaceutical compositions comprising these compounds.
摘要:
This invention relates to process for asymmetrically producing enantiomerically pure .alpha.-cycloalkylalkyl substitututed methanamines from .alpha.-pinene. One key step of the process of this invention utilizes the oxidation product of .alpha.-pinene, hydroxy pinanone, as a chiral auxiliary to direct the stereoselective alkylation of the corresponding ketimine. This invention also relates to key intermediates useful in the processes referred to herein.
摘要:
Disclosed are substituted benzimidazole compounds of formula (I): wherein R1, R2, R3, R4 and Xa are defined herein. The compounds of the invention inhibit Itk kinase and are therefore useful for treating diseases and pathological conditions involving inflammation, immunological disorders and allergic disorders. Also disclosed are processes for preparing these compounds and to pharmaceutical compositions comprising these compounds.
摘要:
Disclosed is an apparatus for automated synthesis containing a shaker deck with a plurality of reaction blocks containing a plurality of reaction wells, an arm containing an array of extending units capable of actuating physical steps along a plurality of axes of each reaction block, each reaction block being situated on a turntable, each turntable being further capable of rotating the reaction block along a central axis. Also disclosed are methods of preparing a peptide, oligonucleotide an small molecules using the apparatus.
摘要:
Disclosed are compounds of formula(I): wherein Ar1, Ar2, R1, R2, R3, R4 and Xa are defined herein. The compounds of the invention inhibit Itk kinase and are therefore useful for treating diseases and pathological conditions involving inflammation, immunological disorders and allergic disorders. Also disclosed are processes for preparing these compounds and to pharmaceutical compositions comprising these compounds.
摘要翻译:公开了式(I)的化合物:其中Ar 1,Ar 2,R 1,R 2, R 3,R 4和X a a在本文中定义。 本发明的化合物抑制Itk激酶,因此可用于治疗涉及炎症,免疫学障碍和过敏性疾病的疾病和病理状况。 还公开了制备这些化合物的方法和包含这些化合物的药物组合物。