- One-pot directed alkylation/deprotection strategy for the synthesis of substituted pyrrole[3,4-d]pyridazinones
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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
- Nair, Reji N.,Bannister, Thomas D.
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- MUSCARINIC M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS
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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).
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Page/Page column 40; 42
(2018/03/25)
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- FLUOROINDOLE DERIVATIVES AS MUSCARINIC M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS
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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)
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Page/Page column 24; 25
(2017/03/28)
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- PYRIDONE DERIVATIVES AND THEIR USE AS KINASE INHIBITORS
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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.
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Page/Page column 188; 189
(2017/05/10)
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- LABELLED CHROMONE DERIVATIVES
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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
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Page/Page column 16; 17
(2016/07/05)
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- INHIBITORS OF HEPATITIS C VIRUS POLYMERASE
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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.
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Paragraph 583; 584
(2016/10/11)
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- HETEROCYCLYL-PYRIDINYL-BASED BIPHOSPHONIC ACID, PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, COMPOSITION THEREOF AND METHOD OF USE THEREOF
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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
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- Discovery of the first non-ATP competitive IGF-1R kinase inhibitors: Advantages in comparison with competitive inhibitors
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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.
- 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
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p. 2224 - 2228
(2011/05/15)
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- PYRANYL ARYL METHYL BENZOQUINAZOLINONE M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS
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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
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Page/Page column 58
(2011/04/14)
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- BENZOXAZINONE DERIVATIVES FOR THE TREATMENT OF GLYTL MEDIATED DISORDERS
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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.
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Page/Page column 66
(2011/02/24)
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- Generation and intermodular additions of pyridylmethyl radicals
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2-, 3-, or 4-Pyridylmethyl radicals can be made to add to nonactivated alkenes to give a variety of otherwise inaccessible pyridine derivatives. Bicyclic structures can be obtained by combining the radical addition with ionic ring-closure steps. Georg Thieme Verlag Stuttgart.
- Ferjancic, Zorana,Quiclet-Sire, Beatrice,Zard, Samir Z.
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experimental part
p. 2996 - 3008
(2009/04/07)
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- NOVEL COMPOUND HAVING 4-PYRIDYLALKYLTHIO GROUP AS SUBSTITUENT
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A subject of the present invention is to provide a novel aromatic five- or six-memberd heterocyclic derivative having 4-pyridylalkylthio as a substituent or a salt thereof which is useful as a pharmaceutical. Compound represented by the following general formula [I] or salts thereof are useful as therapeutic agents for diseases in which angiogenesis or augmentation of vascular permeability is involved. In the formula, ring "A" is a benzene ring or an aromatic five- or six-memberd heterocycle which can be fused with a cycloalkane ring, "B" is alkylene, R1 and R2, the same or different, are H, OH, substituted or unsubstituted alkoxy and the like, X and Y, the same or different, are group(s) selected from H, halogen, OH, substituted or unsubstituted alkoxy and the like respectively, p is 0, 1 or 2, and q is 0 or 1.
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Page/Page column 54
(2008/06/13)
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- Novel cyclic urea derivatives, preparation thereof and pharmaceutical use thereof as kinase inhibitors
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The present invention relates to a cyclic urea compound of formula I: as defined herein. The invention is also directed to the process for its preparation, pharmaceutical composition comprising it and its pharmaceutical use, as an inhibitor on a protein kinase. Thus, it is useful for preventing or treating a physiological disorder capable of being modulated by inhibiting the activity of a protein kinase, such as a solid tumor.
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