- OGA INHIBITOR COMPOUNDS
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The present invention relates to O-GlcNAc hydrolase (OGA) inhibitors. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and
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Page/Page column 49
(2021/06/26)
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- Substituted benzimidazoles as modulators of Ras signaling
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Benzimidazole compounds that increase the rate of SOS-mediated nucleotide exchange on Ras by binding to a functionally relevant, chemically tractable pocket on the SOS protein, as part of the Ras:SOS:Ras complex.
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Page/Page column 211-213; 213-215; 219-220; 221-223; 225-227
(2019/12/25)
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- COMPOSITIONS AND METHODS USING THE SAME FOR TREATMENT OF NEURODEGENERATIVE AND MITOCHONDRIAL DISEASE
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The present disclosure is directed, in part, to compounds, or pharmaceutically acceptable salts thereof, for the treatment and/or prevention of neurodegenerative disease, mitchonodrial disease, fibrosis, and/or cardiomyopathy.
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Paragraph 0265
(2019/01/10)
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- Discovery of imigliptin, a novel selective DPP-4 inhibitor for the treatment of type 2 diabetes
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We report our discovery of a novel series of potent and selective dipeptidyl peptidase IV (DPP-4) inhibitors. Starting from a lead identified by scaffold-hopping approach, our discovery and development efforts were focused on exploring structure-activity relationships, optimizing pharmacokinetic profile, improving in vitro and in vivo efficacy, and evaluating safety profile. The selected candidate, Imigliptin, is now undergoing clinical trial.
- Shu, Chutian,Ge, Hu,Song, Michael,Chen, Jyun-Hong,Zhou, Huimin,Qi, Qu,Wang, Feng,Ma, Xifeng,Yang, Xiaolei,Zhang, Genyan,Ding, Yanwei,Zhou, Dapeng,Peng, Peng,Shih, Cheng-Kon,Xu, Jun,Wu, Frank
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supporting information
p. 921 - 926
(2014/09/17)
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- FUSED PYRIDINE DERIVATIVES
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Fused pyridine derivatives shown as the general formula (I), and their pharmaceutically acceptable salts, stereoisomers or solvates thereof are disclosed, which belong to the technical field of medicines. The R1, R2, R3, Q, X and Y substituents in formula (I) are defined as in the description. Also disclosed are the preparation methods, pharmaceutical compositions comprising the compounds and uses of the compounds in the manufacture of the medicine for the treatment and/or prevention of noninsulin-dependent diabetes, hyperglycemia, hyperlipidemia and insulin resistance.
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Page/Page column 40
(2012/12/13)
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- FUSED PYRIDINE DERIVATIVES
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Fused pyridine derivatives shown as the general formula (I), and their pharmaceutically acceptable salts, stereoisomers or solvates thereof are disclosed, which belong to the technical field of medicines. The R1, R2, R3, Q, X and Y substituents in formula (I) are defined as in the description. Also disclosed are the preparation methods, pharmaceutical compositions comprising the compounds and uses of the compounds in the manufacture of the medicine for the treatment and/or prevention of noninsulin-dependent diabetes, hyperglycemia, hyperlipidemia and insulin resistance.
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Page/Page column 43-44
(2012/12/13)
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- 1- (1-CYCLOHEXYL-4-PIPERIDINYL) -1, 3-DIHYDRO-2H-BENZIMIDAZOL-2-ONE DERIVATIVES WHICH HAVE ACTIVITY ON THE M1 RECEPTOR AND THEIR USE IN MEDICINE
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Compounds of formula (I) or a salt thereof are provided, wherein X1, X2, X3, R6, Q and R are as defined in the description. Uses of the compounds as medicaments and in the manufacture of medicaments for treating
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Page/Page column 65
(2008/12/04)
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- Dihydropyrrole[2,3-d]pyridine derivatives as novel corticotropin-releasing factor-1 antagonists: Mapping of the receptor binding pocket by in silico docking studies
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In an effort to discover novel CRF-1 receptor antagonists exhibiting improved physicochemical properties, a dihydropirrole[2,3]pyridine scaffold was designed and explored in terms of the SAR of the substitution at the pendent phenyl ring and the nature of
- Di Fabio, Romano,Arban, Roberto,Bernasconi, Giovanni,Braggio, Simone,Blaney, Frank E.,Capelli, Anna M.,Castiglioni, Emiliano,Donati, Daniele,Fazzolari, Elettra,Ratti, Emiliangelo,Feriani, Aldo,Contini, Stefania,Gentile, Gabriella,Ghirlanda, Damiano,Sabbatini, Fabio M.,Andreotti, Daniele,Spada, Simone,Marchioro, Carla,Worby, Angela,St-Denis, Yves
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experimental part
p. 7273 - 7286
(2009/11/30)
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- 2-n-butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization
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Two types of adenosine receptor ligands were designed, i.e., 9H-purine and 1H-imidazo[4,5-c]pyridines, to obtain selective A2A antagonists, and we report here their synthesis and binding affinities for the four adenosine receptor subtypes Asub
- Minetti, Patrizia,Tinti, Maria Ornella,Carminati, Paolo,Castorina, Massimo,Di Cesare, Maria Assunta,Di Serio, Stefano,Gallo, Grazia,Ghirardi, Orlando,Giorgi, Fabrizio,Giorgi, Luca,Piersanti, Giovanni,Bartoccini, Francesca,Tarzia, Giorgio
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p. 6887 - 6896
(2007/10/03)
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- Design and synthesis of tricyclic imidazo[4,5-b]pyridin-2-ones as corticotropin-releasing factor-1 antagonists
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The synthesis and SAR studies of tricyclic imidazo[4,5-b]pyridin-2-ones as human corticotropin-releasing factor receptor (CRF1) antagonists are discussed herein. Compound 16g was identified as a functional antagonist that inhibited CRF-stimulat
- Guo, Zhiqiang,Tellew, John E.,Gross, Raymond S.,Dyck, Brian,Grey, Jonathan,Haddach, Mustapha,Kiankarimi, Mehrak,Lanier, Marion,Li, Bin-Feng,Luo, Zhiyong,McCarthy, James R.,Moorjani, Manisha,Saunders, John,Sullivan, Robert,Zhang, Xiaohu,Zamani-Kord, Said,Grigoriadis, Dimitri E.,Crowe, Paul D.,Chen, Ta Kung,Williams, John P.
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p. 5104 - 5107
(2007/10/03)
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- Ether substituted imidazopyridines
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Imidazopyridine compounds that contain an ether or thioether functionality at the 1-position are useful as immune response modifiers. The compounds and compositions of the invention can induce the biosynthesis of various cytokines and are useful in the treatment of a variety of conditions including viral diseases and neoplastic diseases. Methods of preparing the compounds and intermediates useful in the preparation of the compounds are also disclosed.
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- Amide substituted imidazopyridines
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Imidazopyridine compounds that contain amide functionality at the 1-position are useful as immune response modifiers. The compounds and compositions of the invention can induce the biosynthesis of various cytokines and are useful in the treatment of a variety of conditions including viral diseases and neoplastic diseases.
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- Urea substituted imidazopyridines
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Imidazopyridine compounds that contain urea or thiourea functionality at the 1-position are useful as immune response modifiers. The compounds and compositions of the invention can induce the biosynthesis of various cytokines and are useful in the treatment of a variety of conditions including viral diseases and neoplastic diseases.
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- Process for imidazo[4,5-c]pyridin-4-amines
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A process and intermediates for preparing 1H-imidazo[4,5-c]pyridin-4-amines are disclosed. The process includes providing a 4-phenoxy-1H-imidazo[4,5-c]pyridine and aminating the 4-phenoxy-1H-imidazo[4,5-c]pyridine to provide a 1H-imidazo[4,5-c]pyridin-4-a
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- Sulfonamido substituted imidazopyridines
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Imidazopyridine compounds that contain sulfonamide functionality at the 1-position are useful as immune response modifiers. The compounds and compositions of the invention can induce the biosynthesis of various cytokines and are useful in the treatment of a variety of conditions including viral diseases and neoplastic diseases.
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- CRF receptor antagonists and methods relating thereto
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Compounds are disclosed which have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in a warm-blooded animals, including stroke. The compounds of this invention have the following structures: wherein n, m, R, R1, R2, X and Ar are as defined herein, including stereoisomes and pharmaceutically acceptable salts thereof.
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Page column 16
(2010/01/30)
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- Thermal cyclization of 4-azido-3-nitropyridines to furoxanes [1]
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4-Chloro-3-nitro-2-pyridines 3 and 10, obtained from 4-hydroxy-2-pyridones 1 and 8 after nitration and chlorination, gave with sodium azide 4-azido-3-nitropyridines 4 and 11, which cyclized on thermolysis to furoxans 6 and 12. Desoxygenation of the furoxa
- Stadlbauer,Fiala,Fischer,Hojas
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p. 1253 - 1256
(2007/10/03)
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- 1N-alkyl-N-arylpyrimidinamines and derivatives thereof
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The present invention provides novel compounds, compounds and pharmaceutical compositions thereof, and methods of using same in the treatment of affective disorders, anxiety, depression, post-traumatic stress disorders, eating disorders, supranuclear palsy, irritable bowel syndrome, immune suppression, Alzheimer's disease, gastrointestinal diseases, anorexia nervosa, drug and alcohol withdrawal symptoms, drug addiction, inflammatory disorders, or fertility problems. The novel compounds provided by this invention are those of formula: wherein R1, R3, R4, R5, Z, Y, V, X, X', J, K, L, and M are as defined herein.
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- Arylamino fused pyrimidines
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Corticotropin releasing factor (CRF) antagonists of formula I or formula II: and their use in treating anxiety, depression, and other psychiatric and neurological disorders.
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- Purin-8-ones as corticotropin-releasing hormone (CRH-R1) receptor antagonists
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A series of purin-8-ones was prepared and discovered to have excellent binding affinity to the CRH-R1 receptor. Structure-activity studies focused on amine side-chain optimization, urea substitution and pyridyl isostere incorporation. Thus, the highly potent purin-8-ones show promise as a new class of potential anxiolytics and/or antidepressants.
- Beck, James P.,Arvanitis, Argyrios G.,Curry, Matt A.,Rescinito, Joseph T.,Fitzgerald, Larry W.,Gilligan, Paul J.,Zaczek, Robert,Trainor, George L.
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p. 967 - 972
(2007/10/03)
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- Synthesis, corticotropin-releasing factor receptor binding affinity, and pharmacokinetic properties of triazolo-, imidazo-, and pyrrolopyrimidines and -pyridines
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The synthesis and CRF receptor binding affinities of several new series of N-aryltriazolo- and -imidazopyrimidines and -pyridines are described. These cyclized systems were prepared from appropriately substituted diaminopyrimidines or -pyridines by nitrous acid, orthoester, or acyl halide treatment. Variations of amino (ether) pendants and aromatic substituents have defined the structure-activity relationships of these series and resulted in the identification of a variety of high-affinity agents (K(i)'s 1 has been selected for further pharmacological studies that will be reported in due course.
- Chorvat, Robert J.,Bakthavatchalam, Rajagopal,Beck, James P.,Gilligan, Paul J.,Wilde, Richard G.,Cocuzza, Anthony J.,Hobbs, Frank W.,Cheeseman, Robert S.,Curry, Matthew,Rescinito, Joseph P.,Krenitsky, Paul,Chidester, Dennis,Yarem, Jerry A.,Klaczkiewicz, John D.,Hodge, C. Nicholas,Aldrich, Paul E.,Wasserman, Zelda R.,Fernandez, Christine H.,Zaczek, Robert,Fitzgerald, Lawrence W.,Huang, Shiew-Mei,Shen, Helen L.,Wong, Y. Nancy,Chien, Ben M.,Quon, Check Y.,Arvanitis, Argyrios
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p. 833 - 848
(2007/10/03)
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