Patent classifications
C07C233/10
PROCESS FOR THE PREPARATION OF BIMATOPROST
It is provided a process for the preparation of bimatoprost, which comprises: a) reacting a compound of formula (III) with ethylamine in the presence of a suitable solvent; and b) deprotecting compound obtained in step a) to obtain bimatoprost, wherein R.sup.1 is selected from (C.sub.1-C.sub.16)alkyl, (C.sub.1C.sub.16)haloalkyl, (C.sub.2-C.sub.16)alkenyl, (C.sub.2-C.sub.16)haloalkenyl, (C.sub.1-C.sub.16)alkoxy(C.sub.1-C.sub.16)alkyl, aryl, (C.sub.1-C.sub.16)alkylaryl, allyl, (CH.sub.2CH.sub.2O).sub.nCH.sub.3 wherein n=1, 2, 3 or 4, and CH(OCH.sub.2CH.sub.2).sub.2; R.sub.2 is selected from H, (C.sub.1-C.sub.16)alkyl, (C.sub.1-C.sub.16)haloalkyl, (C.sub.2-C.sub.16)alkenyl, (C.sub.2-C.sub.16)haloalkenyl, (C.sub.1-C.sub.16)alkoxy(CrC.sub.16)alkyl, aryl, (C.sub.1-C.sub.16)alkylaryl, allyl; or, alternatively, R.sup.1 and R.sup.2 taken together are selected from CH.sub.2CH.sub.2CH.sub.2, CH.sub.2CH.sub.2, OCH.sub.2CH.sub.2, and OCHCH. There are also provided intermediates useful in such preparation process.
##STR00001##
PROCESS FOR THE PREPARATION OF BIMATOPROST
It is provided a process for the preparation of bimatoprost, which comprises: a) reacting a compound of formula (III) with ethylamine in the presence of a suitable solvent; and b) deprotecting compound obtained in step a) to obtain bimatoprost, wherein R.sup.1 is selected from (C.sub.1-C.sub.16)alkyl, (C.sub.1C.sub.16)haloalkyl, (C.sub.2-C.sub.16)alkenyl, (C.sub.2-C.sub.16)haloalkenyl, (C.sub.1-C.sub.16)alkoxy(C.sub.1-C.sub.16)alkyl, aryl, (C.sub.1-C.sub.16)alkylaryl, allyl, (CH.sub.2CH.sub.2O).sub.nCH.sub.3 wherein n=1, 2, 3 or 4, and CH(OCH.sub.2CH.sub.2).sub.2; R.sub.2 is selected from H, (C.sub.1-C.sub.16)alkyl, (C.sub.1-C.sub.16)haloalkyl, (C.sub.2-C.sub.16)alkenyl, (C.sub.2-C.sub.16)haloalkenyl, (C.sub.1-C.sub.16)alkoxy(CrC.sub.16)alkyl, aryl, (C.sub.1-C.sub.16)alkylaryl, allyl; or, alternatively, R.sup.1 and R.sup.2 taken together are selected from CH.sub.2CH.sub.2CH.sub.2, CH.sub.2CH.sub.2, OCH.sub.2CH.sub.2, and OCHCH. There are also provided intermediates useful in such preparation process.
##STR00001##
COMPOUND FOR CAPPING LAYER AND ORGANIC LIGHT EMITTING DEVICE INCLUDING SAME
A novel compound for a capping layer, and an organic light-emitting device containing the same are disclosed.
COMPOUND FOR CAPPING LAYER AND ORGANIC LIGHT EMITTING DEVICE INCLUDING SAME
A novel compound for a capping layer, and an organic light-emitting device containing the same are disclosed.
IMMUNOREGULATORY AGENTS
- Hilary Plake Beck ,
- Juan Carlos Jaen ,
- Maksim Osipov ,
- Jay Patrick Powers ,
- Maureen Kay Reilly ,
- Hunter Paul Shunatona ,
- James Ross Walker ,
- Mikhail Zibinsky ,
- James Aaron Balog ,
- David K. Williams ,
- Jay A. Markwalder ,
- Steven P. Seitz ,
- Emily Charlotte Cherney ,
- Liping Zhang ,
- Weifang Shan ,
- Weiwei Guo ,
- Audris Huang
Compounds that modulate the oxidoreductase enzyme indoleamine 2,3-dioxygenase, and compositions containing the compounds, are described herein. The use of such compounds and compositions for the treatment and/or prevention of a diverse array of diseases, disorders and conditions, including cancer- and immune-related disorders, that are mediated by indoleamine 2,3-dioxygenase is also provided.
Non-Lactone Carbocyclic and Heterocyclic Antagonists and Agonists of Bacterial Quorum Sensing
Non-lactone carbocyclic and heterocyclic antagonists and agonists of bacterial quorum sensing. Pharmaceutical composition containing antagonists. Methods employing antagonists and agonists for modulation of quorum sensing. Compounds are exemplified by those of formula:
A-[Z].sub.n-L1-[Y].sub.q-W-[V].sub.m-L2-HG,
where A is an acyclic aliphatic group, and HG is an optionally substituted phenyl group. Compounds include those where m and n are both 0, W is NH, Y is present and is COCH.sub.2CO, and L1 and L2 independently are [CH.sub.2].sub.p1 and [CH.sub.2].sub.p2, where p1 and p2, independently, are 0 or integers ranging from 1-10.
N-(5-arylamido-2-methylphenyl)-5-methylisooxazole-4-carboxamide deravative, pharmaceutical acceptable salt thereof, method for preparation therof and FMS kinase inhibitor comprising the same as anactive ingredient
The present invention relates to N-(5-arylamido-2-methylphenyl)-5-methylisoquoxazole-4-carboxamide derivative, or a pharmaceutically acceptable salt thereof and a pharmaceutical composition comprising same. The compound according to the present invention exhibits an FMS kinase inhibitory activity and thus can be used as pharmaceutical composition for preventing and treating diseases associated therewith.
N-(5-arylamido-2-methylphenyl)-5-methylisooxazole-4-carboxamide deravative, pharmaceutical acceptable salt thereof, method for preparation therof and FMS kinase inhibitor comprising the same as anactive ingredient
The present invention relates to N-(5-arylamido-2-methylphenyl)-5-methylisoquoxazole-4-carboxamide derivative, or a pharmaceutically acceptable salt thereof and a pharmaceutical composition comprising same. The compound according to the present invention exhibits an FMS kinase inhibitory activity and thus can be used as pharmaceutical composition for preventing and treating diseases associated therewith.
γ-aminobutyric acid (GABA) analogues for the treatment of pain and other disorders
A compound of Formula 1 ##STR00001## wherein R.sub.1 represents hydrogen, halo, a C1-C4 alkyl group, a C1-C4 alkylhalide group, a C1-C4 alkoxy-C2-C4 alkyl group, a C2-C4 alkenyl group, a C2-C4 alkynyl group or a C3-C7 cycloalkyl group; R.sub.2 represents ##STR00002##
or a tautomer thereof; and R.sub.3 represents hydrogen, a C1-C4 alkyl group, a C1-C4 alkoxy-C2-C4 alkyl group or a C3-C7 cycloalkyl group; or a pharmaceutically acceptable salt or solvate thereof. Processes to prepare said compounds and novel intermediates are also claimed. Such compound finds utility in treating neuropathic pain and disorders of the central nervous system.
γ-aminobutyric acid (GABA) analogues for the treatment of pain and other disorders
A compound of Formula 1 ##STR00001## wherein R.sub.1 represents hydrogen, halo, a C1-C4 alkyl group, a C1-C4 alkylhalide group, a C1-C4 alkoxy-C2-C4 alkyl group, a C2-C4 alkenyl group, a C2-C4 alkynyl group or a C3-C7 cycloalkyl group; R.sub.2 represents ##STR00002##
or a tautomer thereof; and R.sub.3 represents hydrogen, a C1-C4 alkyl group, a C1-C4 alkoxy-C2-C4 alkyl group or a C3-C7 cycloalkyl group; or a pharmaceutically acceptable salt or solvate thereof. Processes to prepare said compounds and novel intermediates are also claimed. Such compound finds utility in treating neuropathic pain and disorders of the central nervous system.