29421-72-5Relevant academic research and scientific papers
Highly reactive bis-cyclooctyne-modified diarylethene for SPAAC-mediated cross-linking
Strizhak, Alexander V.,Sharma, Krishna,Spring, David R.,Babii, Oleg,Afonin, Sergii,Ulrich, Anne S.,Komarov, Igor V.
, p. 8559 - 8564 (2018)
Photoisomerizable diarylethenes equipped with triple bonds are promising building blocks for constructing bistable photocontrollable systems. Here we report on the design, synthesis and application of a cross-linking reagent which is based on a diarylethene core and features two strained cyclooctynes. High reactivity of the cyclooctyne rings in catalyst-free 1,3-dipolar cycloaddition reactions was suggested to stem from the additional strain imposed by the fused thiophene rings. This hypothesis was confirmed by quantum chemical calculations.
MACROCYCLES AS PDE1 INHIBITORS
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, (2019/06/30)
The present invention provides macrocycles of formula (I) as PDE1 inhibitors and their use as a medicament, in particular for the treatment of neurodegenerative disorders and psychiatric disorders.
1H-PYRAZOLO[4,3-B]PYRIDINES AS PDE1 INHIBITORS
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, (2019/07/10)
The present invention provides 1H-pyrazolo[4,3-b]pyridines of formula (I) as PDE1 inhibitors and their use as a medicament, in particular for the treatment of neurodegenerative disorders and psychiatric disorders.
COMBINATION TREATMENTS COMPRISING ADMINISTRATION OF 1H-PYRAZOLO[4,3-B]PYRIDINES
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, (2019/07/19)
The present invention provides 1H-pyrazolo[4,3-b]pyridin-7-amines of formula (I) as PDE1 inhibitors together with a second compound useful in the treatment of a neurodegenerative disorder and their combined use as a medicament, in particular for the treatment of neurodegenerative and/or cognitive disorders.
COMBINATION TREATMENTS COMPRISING ADMINISTRATION OF 1H-PYRAZOLO[4,3-B]PYRIDINES
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, (2019/07/19)
The present invention provides 1H-pyrazolo[4,3-b]pyridin-7-amines of formula (I) as PDE1 inhibitors together with a second compound which compound is useful in the treatment of a psychiatric disorder and their combined use as a medicament, in particular for the treatment of psychiatric and/or cognitive disorders.
Peptidylarginine deiminase inhibitor and application thereof
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Paragraph 0500-0504; 0802; 0804; 0805; 0806; 0807; 0808, (2019/09/10)
The invention belongs to the technical field of medicine, and particularly relates to a peptidylarginine deiminase PAD4 inhibitor compound shown in a formula (I) or pharmaceutically acceptable salts,stereoisomers and tautomers thereof, as well as pharmaceutical compositions, pharmaceutical preparations and application thereof. X, Y, R1, R2, R3, R4, R5, R7, R8, R9, ring B and m are as defined in the specification. The compound has inhibitory effect on peptidylarginine deiminase PAD4, and can be used for treating various diseases, such as rheumatoid arthritis, vasculitis, systemic lupus erythematosus, ulcerative colitis, multiple sclerosis, cystic fibrosis, cancer, cutaneous lupus erythematosus, asthma and psoriasis.
1H-PYRAZOLO[4,3-B]PYRIDINES AS PDE1 INHIBITORS
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, (2018/09/25)
The present invention provides 1H-pyrazolo[4,3-b]pyridin-7-amines of formula (I) as PDE1 inhibitors and their use as a medicament, in particular for the treatment of neurodegenerative disorders and psychiatric disorders.
Lithiation of Heterocycles Directed by α-Amino Alkoxides
Comins, Daniel L.,Killpack, Michael O.
, p. 104 - 109 (2007/10/02)
The addition of heterocyclic aromatic aldehydes to certain lithium dialkylamides gave α-amino alkoxides that were ring-lithiated with butyllithium.Alkylation and hydrolysis provided ring-substituted heterocyclic aromatic aldehydes via a one-pot reaction.The metalation of α-amino alkoxides derived from thiophenecarboxaldehydes, furaldehydes, N-methylpyrrolecarboxaldehydes, and indolecarboxaldehydes was examined.The regioselectivity of the lithiation, was dependent on the heterocycle, the amine component of the α-amino alkoxide, and the metalation conditions.A novel N-methyl metalation of α-amino alkoxides derived from N-methylpyrrole-2-carboxaldehyde and N-methylindole-2-carboxaldehyde was achieved when N,N,N'-trimethylethylenediamine was used as the amine component for in situ formation of the α-amino alkoxides.The novel directed N-methyl lithiations are attributed to an intramolecular TMEDA-like assisted metalation.
