- New fluorescent tetraphenylporphyrin-based dendrimers with alkene-linked fluorenyl antennae designed for oxygen sensitization
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The design of porphyrin-based dendrimers featuring conjugated fluorenyl dendrons via alkene spacers allows evaluating the importance of the role of these spacers on the optical properties of interest. In the continuation of previous studies, a second-gene
- Blanchard-Desce, Mireille,Mongin, Olivier,Paul, Frédéric,Paul-Roth, Christine O.,Shi, Limiao,Sun, Zhipeng,Yao, Dandan
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- Novel phenanthrene compounds, a method of making the same and organic electronic devices using the same
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The present invention relates to novel phenanthrene compounds having excellent luminous efficiency and lifespan, a manufacturing method thereof, and an organic electronic device including the novel phenanthrene compounds. The novel phenanthrene compounds according to the present invention can form steric conformation, can improve performance through improvement of electronic density, also can improve performance by regulating the molecular weight and position of a functional group because the molecular weight of the compounds is low, and can minutely regulate luminous wavelength and improve performance according to types of the functional groups. As the result, the organic electronic device including the novel phenanthrene compounds has high brightness, excellent thermal resistance, long lifespan, and high efficiency.
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Paragraph 0236-0239; 0476-0479
(2019/10/22)
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- Exploration of phenylpropanoic acids as agonists of the free fatty acid receptor 4 (FFA4): Identification of an orally efficacious FFA4 agonist
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The long chain free fatty acid receptor 4 (FFA4/GPR120) has recently been recognized as lipid sensor playing important roles in nutrient sensing and inflammation and thus holds potential as a therapeutic target for type 2 diabetes and metabolic syndrome. To explore the effects of stimulating this receptor in animal models of metabolic disease, we initiated work to identify agonists with appropriate pharmacokinetic properties to support progression into in vivo studies. Extensive SAR studies of a series of phenylpropanoic acids led to the identification of compound 29, a FFA4 agonist which lowers plasma glucose in two preclinical models of type 2 diabetes.
- Sparks, Steven M.,Aquino, Christopher,Banker, Pierette,Collins, Jon L.,Cowan, David,Diaz, Caroline,Dock, Steven T.,Hertzog, Donald L.,Liang, Xi,Swiger, Erin D.,Yuen, Josephine,Chen, Grace,Jayawickreme, Channa,Moncol, David,Nystrom, Christopher,Rash, Vincent,Rimele, Thomas,Roller, Shane,Ross, Sean
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p. 1278 - 1283
(2017/06/19)
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- ANILINE DERIVATIVES,THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION
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The present invention relates to aniline derivatives, to their preparation and to their therapeutic application.
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Page/Page column 55
(2013/03/28)
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- Regioisomerism in the synthesis of a chiral aminotetralin drug compound: Unraveling mechanistic details and diastereomer-specific in-depth NMR investigations
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During chemical process development of a novel 2-aminotetralin derivative intended for use as an antidepressant, scrutiny of the byproduct present in the drug molecule revealed a set of regioisomers. Detailed studies showed that this impurity issue origin
- Schuisky, Peter,Federsel, Hans-Juergen,Tian, Wei
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experimental part
p. 5503 - 5514
(2012/09/07)
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- Dual Pharmacophores - PDE4-Muscarinic Antagonistics
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The present invention relates to novel compounds of Formula (I) and their use in the treatment of respiratory diseases, including anti-inflammatory and allergic diseases such as chronic obstructive pulmonary disease (COPD), asthma, rhinitis (e.g. allergic rhinitis), atopic dermatitis or psoriasis.
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Page/Page column 50; 51
(2009/08/18)
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- Dual Pharmacophores - PDE4-Muscarinic Antagonistics
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The present invention is directed to novel compounds of Formula (I), pharmaceutical compositions and their use in therapy, for example as inhibitors of phosphodiesterase type IV (PDE4) and as antagonists of muscarinic acetylcholine receptors (mAChRs), in the treatment of/and or prophylaxis of respiratory diseases, including antiinflammatory and/or allergic diseases such as chronic obstructive pulmonary disease (COPD), asthma, rhinitis (e.g. allergic rhinitis), atopic dermatitis or psoriasis.
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Page/Page column 50
(2009/08/16)
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- DUAL PHARMACOPHORES - PDE4-MUSCARINIC ANTAGONISTICS
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The present invention is directed to novel compounds of Formula's (I) - (VI), and pharmaceutically acceptable salts thereof, pharmaceutical compositions and their use in therapy, for example as inhibitors of phosphodiesterase type IV (PDE4) and as antagonists of muscarinic acetylcholine receptors (mAChRs), in the treatment of and/or prophylaxis of respiratory diseases, including inflammatory and/or allergic diseases such as chronic obstructive pulmonary disease (COPD), asthma, rhinitis (e.g. allergic rhinitis), atopic dermatitis or psoriasis.
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Page/Page column 126
(2009/10/09)
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- NOVEL HIV REVERSE TRANSCRIPTASE INHIBITORS
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The invention is related to compounds of Formula (I) or a pharmaceutically acceptable salt, solvate, ester, and/ or phosphonate thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.
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Page/Page column 383
(2009/03/07)
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- PROCESSES FOR PREPARING HIV REVERSE TRANSCRIPTASE INHIBITORS
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Compounds of Formula (I): can be prepared by a multi-step process from compounds of Formula (II): wherein G is Cl, Br or I.
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Page/Page column 13-14; 18-19
(2009/07/10)
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- Dual Pharmacophores - PDE4-Muscarinic Antagonistics
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The present invention is directed to novel compounds of Formula (I) and pharmaceutically acceptable salts thereof, pharmaceutical compositions and their use as dual chromaphores having inhibitory activity against PDE4 and muscarinic acetylcholine receptors (mAChRs), and thus being useful for treating respiratory diseases.
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Page/Page column 47-48
(2009/08/18)
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- Novel HIV reverse transcriptase inhibitors
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The invention is related to compounds of Formula (I), (II), or (III): or a pharmaceutically acceptable salt, solvate, ester, and/or phosphonate thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.
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Page/Page column 34-35; 66-67
(2008/06/13)
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- SPIRO IMIDAZOLE DERIVATIVES AS PPAR MODULATORS
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The invention provides compounds (Ia), (Ib) and (Ic), pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of the Peroxisome Proliferator-Activated
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Page/Page column 42
(2008/06/13)
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- Dual aromatase-sulfatase inhibitors based on the anastrozole template: Synthesis, in vitro SAR, molecular modelling and in vivo activity
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The synthesis and biological evaluation of a series of novel Dual Aromatase-Sulfatase Inhibitors (DASIs) are described. It is postulated that dual inhibition of the aromatase and steroid sulfatase enzymes, both responsible for the biosynthesis of oestrogens, will be beneficial in the treatment of hormone-dependent breast cancer. The compounds are based upon the Anastrozole aromatase inhibitor template which, while maintaining the haem ligating triazole moiety crucial for enzyme inhibition, was modified to include a phenol sulfamate ester motif, the pharmacophore for potent irreversible steroid sulfatase inhibition. Adaption of a synthetic route to Anastrozole was accomplished via selective radical bromination and substitution reactions to furnish a series of inhibitory aromatase pharmacophores. Linking these fragments to the phenol sulfamate ester moiety employed SN2, Heck and Mitsunobu reactions with phenolic precursors, from where the completed DASIs were achieved via sulfamoylation. In vitro, the lead compound, 11, had a high degree of potency against aromatase (IC50 3.5 nM), comparable with that of Anastrozole (IC50 1.5 nM) whereas, only moderate activity against steroid sulfatase was found. However, in vivo, 11 surprisingly exhibited potent dual inhibition. Compound 11 was modelled into the active site of a homology model of human aromatase and the X-ray crystal structure of steroid sulfatase. This journal is The Royal Society of Chemistry.
- Jackson, Toby,Woo, L. W. Lawrence,Trusselle, Melanie N.,Chander, Surinder K.,Purohit, Atul,Reed, Michael J.,Potter, Barry V. L.
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p. 2940 - 2952
(2008/04/02)
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- 1,2,4-TRIAZOL-l-YL BISPHENYL DERIVATIVES FOR USE IN THE TREATMENT OF ENDOCRINE-DEPENDENT TUMOURS
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There is provided a compound of Formula I wherein R3, R4, R5, R6 and R7 are independently selected from H and -Y-R6; wherein each R8 is independently selected from -OH, hydrocarbyl groups, oxyhydrocarbyl groups, cyano (-CN), nitro (-NO2), H-bond acceptors, and halogens; wherein at Jeast one of R3, R4, R5, R6 and R7 is -Y-R8 wherein R8 is selected from substituted and unsubstituted ? heterocyclic rings and amino substituted phenyl groups, wherein X is a bond or a linker group; wherein Y is an optional linker group; and wherein ring A is optionally further , substituted; wherein R9 is selected from H, -OH and -OSO2NR1R2; wherein R1 and R2 are independently selected from H and hydrocarbyl; wherein (a) X is a bond and at least one of R3, R4, R5, R6 and R7 is -Y-R8; OR (b) R9 is -OSO2NR1R2 or - OH and four of R3, R4, R5, R6 and R7 are H and one of R3, R4, R5, R6 and R7 is -Y-R8. These compounds inhibit steroid sulphatase and aronatase activity and are useful in the treatment of endocrine-dependent tumours.
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Page/Page column 70
(2008/06/13)
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- PHENYL-SULFAMATES AS AROMATASE INHIBITORS
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There is provided a compound of Formula (I) wherein X, Y and Z are each independently of each other an optional linker group; R, is a ring system; R2 is selected from hydrocarbyl groups, oxyhydrocarbyl groups, cyano (CN), nitro (-NO2) and halogens; R3 and R4 are independently selected from H and hydrocarbyl, ring A and B are independently optionally further substituted.
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Page/Page column 87-88; 137
(2008/06/13)
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- MACROCYCLIC LACTAMS AND PHARMACEUTICAL USE THEREOF
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The present invention relates to novel macrocyclic compounds of the formula (I) wherein R1, R2, R3, U, V, W, X, Y, Z and n are as defined in the specification, the number of ring atoms included in the macrocyclic ring being 14, 15, 16 or 17, in free base form or in acid addition salt form, to their preparation, to their use as pharmaceuticals and to pharma-ceutical compositions comprising them.
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Page/Page column 65
(2008/06/13)
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- Quinolinone derivaties and uses thereof
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The invention provides compounds of the formula: and pharmaceutically acceptable salts or prodrugs thereof, wherein m, p, q, r, A, E, X, Y, R1, R4, R5, R6, R7, R8, R9 and are as defined herein. The invention also provides methods for preparing, compositions comprising, and methods for using compounds of formula I.
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Page/Page column 22
(2008/06/13)
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- Amine derivatives
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The present invention relates to amine derivatives represented by formula (1) or salts thereof. R3represents C1-C3 alkyl, hydroxylated C1-C5 alkyl, C1-C5 acyl; C2-C5 alkenyl, or a halogen atom; and k, l, and m are each an integer of 1 to 4.) Exhibiting excellent antifungal effect, these compounds are highly useful as antifungal agents, antifungal compositions, drugs, etc.
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- META-GUANIDINE, UREA, THIOUREA OR AZACYCLIC AMINO BENZOIC ACID DERIVATIVES AS INTEGRIN ANTAGONISTS
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The present invention relates to a class of compounds represented by the Formula Ior a pharmaceutically acceptable salt thereof, whereinA ispharmaceutical compositions thereof and methods of using such compounds and compositions as alphavbeta3 antagonists.
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