- HETEROCYCLIC COMPOUNDS AS KINASE INHIBITORS
-
Heterocyclic compounds as CDK4 or CDK6 or other CDK inhibitors are provided. The compounds may find use as therapeutic agents for the treatment of diseases and may find particular use in oncology.
- -
-
Paragraph 0381
(2021/01/23)
-
- TRITERPENOIDS WITH HIV MATURATION INHIBITORY ACTIVITY, SUBSTITUTED IN POSITION 3 BY A NON-AROMATIC RING CARRYING A HALOALKYL SUBSTITUENT
-
Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, triterpenoids that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formula I: with X selected from C4-8 cycloalkyl, C4-8 cycloalkenyl, C4-9 spirocycloalkyl, C4-9 spirocycloalkenyl, C4-8 oxacycloalkyl, C4-8 dioxacycloalkyl, C6-8 oxacycloalkenyl, C6-8 dioxacycloalkenyl, C6 cyclodialkenyl, C6 oxacyclodialkenyl, C6-9 oxaspirocycloalkyl and C6-9 oxaspirocycloalkenyl ring, such that X is substituted with A, wherein A is -C1-6 alkyl- halo. These compounds are useful for the treatment of HIV and AIDS.
- -
-
Page/Page column 261; 262
(2015/11/03)
-
- Synthesis of 1-substituted epibatidine analogues and their in vitro and in vivo evaluation as α4β2 nicotinic acetylcholine receptor ligands
-
The highly potent natural alkaloid epibatidine remains a source of inspiration in the search for new analgesic drugs. In this paper, we describe an expansion of our previously reported synthesis of epibatidine analogues, and five synthetic alkaloids chara
- Heugebaert, Thomas S.A.,Van Overtveldt, Melissa,De Blieck, Ann,Wuyts, Benjamin,Augustijns, Patrick,Ponce-Gamez, Eugenia,Rivera, Alicia,De Groote, Dominic,Lefebvre, Romain A.,Wouters, Patrick,Meert, Theo,Devulder, Jacques,Stevens, Christian V.
-
p. 2226 - 2234
(2014/01/06)
-
- A straightforward entry to 7-azabicyclo[2.2.1]heptane-l-carbonitriles in the synthesis of novel epibatidine analogues
-
This paper presents the synthesis of epibatidine analogues by a straightforward one-pot method for the synthesis of 7azabicyclo[2.2.1]heptane-1- carbonitriles, starting from cyclohexanones bearing a leaving group at the 4-position. In situ imine formation
- Heugebaert, Thomas,Van Hevele, Joke,Couck, Wouter,Bruggeman, Vicky,Van Jeught, Sarah Der,Masschelein, Kurt,Stevens, Christian V.
-
supporting information; experimental part
p. 1017 - 1020
(2010/04/25)
-