Patent classifications
C07F9/6561
SALTS OF PRODRUGS OF PIPERAZINE AND SUBSTITUTED PIPERIDINE ANTIVIRAL AGENTS
This invention provides for prodrug Compounds I, pharmaceutical compositions thereof, and their use in treating HIV infection.
##STR00001## wherein: X is C or N with the proviso that when X is N, R.sup.1 does not exist; W is C or N with the proviso that when W is N, R.sup.2 does not exist; V is C; E is hydrogen or a pharmaceutically acceptable salt thereof; and Y is selected from the group consisting of
##STR00002##
Also, this invention provides for intermediate Compounds II useful in making prodrug Compounds I.
##STR00003## wherein: L and M are independently selected from the group consisting of C.sub.1-C.sub.6 alkyl, phenyl, benzyl, trialkylsilyl, -2,2,2-trichloroethoxy and 2-trimethylsilylethoxy.
SALTS OF PRODRUGS OF PIPERAZINE AND SUBSTITUTED PIPERIDINE ANTIVIRAL AGENTS
This invention provides for prodrug Compounds I, pharmaceutical compositions thereof, and their use in treating HIV infection.
##STR00001## wherein: X is C or N with the proviso that when X is N, R.sup.1 does not exist; W is C or N with the proviso that when W is N, R.sup.2 does not exist; V is C; E is hydrogen or a pharmaceutically acceptable salt thereof; and Y is selected from the group consisting of
##STR00002##
Also, this invention provides for intermediate Compounds II useful in making prodrug Compounds I.
##STR00003## wherein: L and M are independently selected from the group consisting of C.sub.1-C.sub.6 alkyl, phenyl, benzyl, trialkylsilyl, -2,2,2-trichloroethoxy and 2-trimethylsilylethoxy.
ISOINDOLINE OR ISOQUINOLINE COMPOUNDS, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
Compounds of formula (I):
##STR00001##
wherein Het, R.sub.3, R.sub.4, R.sub.5, R.sub.7, R.sub.8, R.sub.9, T, p, p′, q, and q′ are as defined in the description.
Medicinal products containing the same which are useful in treating conditions requiring a pro-apoptotic agent.
MACROCYCLIZATION REACTIONS AND INTERMEDIATES USEFUL IN THE SYNTHESIS OF ANALOGS OF HALICHONDRIN B
The invention provides methods for the synthesis of eribulin or a pharmaceutically acceptable salt thereof (e.g., eribulin mesylate) through a macrocyclization strategy. The macrocyclization strategy of the present invention involves subjecting a non-macrocyclic intermediate to a carbon-carbon bond-forming reaction (e.g., an olefination reaction (e.g., Horner-Wadsworth-Emmons olefination), Dieckmann reaction, catalytic Ring-Closing Olefin Metathesis, or Nozaki-Hiyama-Kishi reaction) to afford a macrocyclic intermediate. The invention also provides compounds useful as intermediates in the synthesis of eribulin or a pharmaceutically acceptable salt thereof and methods for preparing the same.
NOVEL 3' END CAPS, 5' END CAPS AND COMBINATIONS THEREOF FOR THERAPEUTIC RNA
The disclosure relates to nucleic acids that contain modifications at the 5′-end, 3′-end or 5′-end and 3′-ends, and compounds that can be used to make the modified nucleic acids arc disclosed. The modified nucleic acids have improved expression, lower immunogenicity and improved stability compared to unmodified nucleic acids.
CHOLINERGIC ENHANCERS WITH IMPROVED BLOOD-BRAIN BARRIER PERMEABILITY FOR THE TREATMENT OF DISEASES ACCOMPANIED BY COGNITIVE IMPAIRMENT
A method for the treatment of a neurodegenerative, psychiatric or neurological disease associated with a cholinergic deficit comprising administering GLN-1062 or a pharmaceutically acceptable salt thereof by nasal administration to a patient in need thereof.
##STR00001##
CHOLINERGIC ENHANCERS WITH IMPROVED BLOOD-BRAIN BARRIER PERMEABILITY FOR THE TREATMENT OF DISEASES ACCOMPANIED BY COGNITIVE IMPAIRMENT
A method for the treatment of a neurodegenerative, psychiatric or neurological disease associated with a cholinergic deficit comprising administering GLN-1062 or a pharmaceutically acceptable salt thereof by nasal administration to a patient in need thereof.
##STR00001##
METHODS OF TREATING NEUROLOGICAL INFLAMMATORY DISORDERS
Methods of treating neurological inflammatory disease or seizures caused by neuroinflammation by administering cPMP are described. Treating neuroinflammatory and neurometabolic diseases with cPMP is described so as to override dyshomeostasis in the MoCo synthesis pathway and control synaptic inhibition in the gephyrin-GABAR pathway. This is a novel strategy for preventing neural circuit dyshomeostasis by stabilizing inhibitory synapses.
Azaindole derivatives and their use as ERK kinase inhibitors
The present invention concerns a compound of formula (I), or one of its pharmaceutically acceptable salts, especially for use as inhibitors of the ERK kinase activity in particular ERK2 activity, it also concerns prodrugs of these compounds. ##STR00001##
Azaindole derivatives and their use as ERK kinase inhibitors
The present invention concerns a compound of formula (I), or one of its pharmaceutically acceptable salts, especially for use as inhibitors of the ERK kinase activity in particular ERK2 activity, it also concerns prodrugs of these compounds. ##STR00001##