83004-15-3Relevant academic research and scientific papers
One-pot directed alkylation/deprotection strategy for the synthesis of substituted pyrrole[3,4-d]pyridazinones
Nair, Reji N.,Bannister, Thomas D.
, p. 1764 - 1770 (2015)
In the course of a structure-activity relationship study of pyrrole[3,4-d]pyridazinones, we optimized conditions for a one-pot directed lithiation/alkylation reaction that also promoted in situ cleavage of a tert-butoxycarbonyl (Boc) protecting group on t
MUSCARINIC M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS
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Page/Page column 40; 42, (2018/03/25)
The present invention relates to compounds of formula (I), or their isotopic forms, stereoisomers, tautomers or pharmaceutically acceptable salt (s) thereof as muscarinic M1 receptor positive allosteric modulators (M1 PAMs). The present invention describes the preparation, pharmaceutical composition and the use of compound formula (I).
FLUOROINDOLE DERIVATIVES AS MUSCARINIC M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS
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Page/Page column 24; 25, (2017/03/28)
The present invention relates to compound of formula (I), or stereoisomers and pharmaceutically acceptable salts as muscarinic M1 receptor positive allosteric modulators. This invention also relates to methods of making such compounds and pharmaceutical compositions comprising such compounds. The compounds of this invention are useful in the treatment of various disorders that are related to muscarinic M1 receptor.(Formula I) (I)
PYRIDONE DERIVATIVES AND THEIR USE AS KINASE INHIBITORS
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Page/Page column 188; 189, (2017/05/10)
Disclosed in the present application is a compound of formula (I) as defined herein as well as a pharmaceutical composition comprising said compound. Further disclosed in the present application is the use of such pharmaceutical compositions for treating diseases, namely inter alia for use in the treatment of cancer, metabolic, inflammatory, autoimmune and viral diseases. The compounds disclosed herein are inhibitors of MNK1 and/or MNK2 kinases.
LABELLED CHROMONE DERIVATIVES
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Page/Page column 16; 17, (2016/07/05)
The present invention relates to compounds having selective binding for MAO-B as compared with MAO-A. The invention also provides radioactive versions of these compounds, and precursor compounds for the synthesis of these radioactive compounds. The radioa
INHIBITORS OF HEPATITIS C VIRUS POLYMERASE
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Paragraph 583; 584, (2016/10/11)
The present invention provides, among other things, compounds represented by the general Formula I: (I) and pharmaceutically acceptable salts thereof, wherein L and A (and further substituents) are as defined in classes and subclasses herein and compositions (e.g., pharmaceutical compositions) comprising such compounds, which compounds are useful as inhibitors of hepatitis C virus polymerase, and thus are useful, for example, as medicaments for the treatment of HCV infection.
HETEROCYCLYL-PYRIDINYL-BASED BIPHOSPHONIC ACID, PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, COMPOSITION THEREOF AND METHOD OF USE THEREOF
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, (2011/12/14)
The present invention relates to novel compounds, compositions containing said compounds and methods for inhibiting human farnesyl pyrophosphate synthase or for the treatment or prevention of disease conditions using said compounds, which may also be useful in the inhibition of FPPS enzymes of microorganisms and protozoan parasites such as the groups of Leishmania, Plasmodium, Trypanosoma, Toxoplasma and Cryptosporidium
PYRANYL ARYL METHYL BENZOQUINAZOLINONE M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS
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Page/Page column 58, (2011/04/14)
The present invention is directed to pyranyl aryl methyl benzoquinazolinone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as ALzheimer?s disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor
Discovery of the first non-ATP competitive IGF-1R kinase inhibitors: Advantages in comparison with competitive inhibitors
Lesuisse, Dominique,Mauger, Jacques,Nemecek, Conception,Maignan, Sébastien,Boiziau, Janine,Harlow, Greg,Hittinger, Augustin,Ruf, Swen,Strobel, Hartmut,Nair, Anil,Ritter, Kurt,Malleron, Jean-Luc,Dagallier, Anne,El-Ahmad, Youssef,Guilloteau, Jean-Pierre,Guizani, Houlfa,Bouchard, Hervé,Venot, Corinne
body text, p. 2224 - 2228 (2011/05/15)
A new series of IGF-1R inhibitors related to hydantoins were identified from a lead originating from HTS. Their noncompetitive property as well as their slow binding characteristics provided a series of compounds with unique selectivity and excellent cellular activities.
BENZOXAZINONE DERIVATIVES FOR THE TREATMENT OF GLYTL MEDIATED DISORDERS
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Page/Page column 66, (2011/02/24)
The present invention relates to benzoxazinone derivatives, processes for their preparation, pharmaceutical compositions and medicaments containing them and to their use in treating disorders mediated by GlyT1, including neurological and neuropsychiatric disorders, in particular psychoses, dementia or attention deficit disorder.
