- Novel highly selective peroxisome proliferator-activated receptor δ (PPARδ) modulators with pharmacokinetic properties suitable for once-daily oral dosing
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Optimization of benzamide PPARδ modulator 1 led to (E)-6-(2-((4-(furan-2-yl)-N-methylbenzamido)methyl)phenoxy)-4-methylhex-4-enoic acid (18), a potent selective PPARδ modulator with significantly improved exposure in multiple species following oral administration.
- Lagu, Bharat,Kluge, Arthur F.,Fredenburg, Ross A.,Tozzo, Effie,Senaiar, Ramesh S.,Jaleel, Mahaboobi,Panigrahi, Sunil K.,Tiwari, Nirbhay K.,Krishnamurthy, Narasimha R.,Takahashi, Taisuke,Patane, Michael A.
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Read Online
- Compound with PPAR delta agonistic activity, pharmaceutical composition and medical application
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The invention discloses a compound with PPAR delta agonistic activity, a pharmaceutical composition and medical application, wherein the structure of the compound is shown as a formula I in the specification. The compound shown in the formula I is a novel
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Paragraph 0142-0146
(2021/03/13)
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- Effective bimetallic composite catalysts for the synthesis of arylated furans and thiophenes in aqueous media
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[Figure not available: see fulltext.] N-(4,6-Dimethylpyrimidin-2-yl)-5-phenylisoxazole-3-carboxamide was used as a ligand for obtaining bimetallic boron-containing heterogeneous catalysts Pd–Ni(Co)–B–L (Ni(Co):Pd = 9:1). The obtained composites were highl
- Bumagin, Nikolay A.,Petkevich, Sergey K.,Kletskov, Alexey V.,Alekseyev, Roman S.,Potkin, Vladimir I.
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- Facile C–H arylation using catalytically active terminal sulfurs of 2 dimensional molybdenum disulfide
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The first methodology of C–H arylation of heteroarene via 2D transition metal dichalcogenides that have catalytically active edge functional groups was described. The terminal sulfur groups could effectively catalyze a formation of an azo-linked intermediate with aryl diazonium salts, leading to produce heteroarenes with good yields. This novel methodology using bulk 2D transition metal dichalcogenides that have catalytically active edge functional groups can apply for various reactions to achieve C–C bond formation in the fields of heterogeneous catalysis that is easily separable, highly reusable, and inexpensive method.
- Hwang, Eunhee,Mi Lee, Sae,Bak, Sora,Min Hwang, Hee,Kim, Hyunjung,Lee, Hyoyoung
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supporting information
p. 3969 - 3973
(2018/10/02)
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- PPAR AGONISTS, COMPOUNDS, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE THEREOF
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Provided herein are compounds of formula (I) useful for the treatment of PPAR-delta related diseases (e.g. mitochondrial diseases, muscular diseases, vascular diseases, demyelinating diseases and metabolic diseases).
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Page/Page column 49
(2016/05/02)
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- PPAR AGONISTS AND METHODS OF USE THEREOF
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Provided herein are deuterated compounds and compositions useful in increasing PPAR5 activity. The compounds and compositions provided herein are useful for the treatment of PPAR5 related diseases (e.g., muscular diseases, vascular disease, demyelinating disease, and metabolic diseases).
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Page/Page column 158
(2016/05/02)
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- High-turnover aminopyridine-based Pd-catalysts for Suzuki-Miyaura reaction in aqueous media
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A high-turnover catalytic system based on commercially available aminopyridines (L) and PdCl2 has been developed for Suzuki-Miyaura reaction in aqueous media. Reactions of arylboronic acids with a wide range of aryl iodides, bromides and chlorides proceeded in the presence of these catalysts for a short time in aqueous media to afford the cross-coupling products in high yields. Furthermore, this protocol allows tolerating a wide range of functional groups.
- Bumagin, Nikolay A.
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- Ascorbic acid as an initiator for the direct C-H arylation of (hetero)arenes with anilines nitrosated in situ
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Ascorbic acid (vitaminC) has been used as a radical initiator in a metal-free direct C-H arylation of (hetero)arenes. Starting from an aniline, the corresponding arenediazonium ion is generated in situ and immediately reduced by vitaminC to an aryl radical that undergoes a homolytic aromatic substitution with a (hetero)arene. Notably, neither heating nor irradiation is required. This procedure is mild, operationally simple, and constitutes a greener approach to arylation. Copyright
- Crisostomo, Fernando Pinacho,Martin, Tomas,Carrillo, Romen
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supporting information
p. 2181 - 2185
(2014/03/21)
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- An effective activation of palladium phosphine complexes in aqueous phase reactions of hetero-aromatic boronic acids with aryl halides
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We have developed a simple and effective method for the activation of palladium phosphine complexes in the Suzuki reaction (TON up to 9800, TOF up to 58800 h-1) by selecting an aqueous reaction medium instead of organic solvents. This method wa
- Bumagin,Veselov,Belov
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- 5-(Naphth-1-yl)- and 5-[(1,1'-biphenyl)-4-yl]isoxazole-3-carbaldehyde oximes: Synthesis, complexes with palladium, and application in catalysis
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1-(Naphth-1-yl)- and 1-[(1,1'-biphenyl)-4-yl-3,4,4-trichloro-3-buten-1-ones were synthesized by acylation of naphthalene and biphenyl with 3,4,4-trichloro-3-butenoyl chloride. Further reaction with hydroxylamine led to 5-(naphth-1-yl)- and 5-[(1,1'-biphen
- Potkin,Bumagin,Zelenkovskii,Petkevich,Livantsov,Golantsov
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p. 1782 - 1792
(2015/01/08)
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- PPAR AGONISTS
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Provided herein are compounds and compositions useful in increasing PPARδ activity. The compounds and compositions provided herein are useful for the treatment of PPARδ related diseases (e.g., muscular diseases, vascular disease, demyelinating disease, and metabolic diseases).
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Page/Page column 124
(2014/10/18)
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- Sensitized photografting of diazonium salts by visible light.
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Visible irradiation of a gold surface dipped into a solution of diversely substituted aryldiazonium salts in the presence of a photosensitizer (Ru(bipy)32+ or eosinY) leads to a modification of the surface by attached aryl groups. A grafted nanometer thick polyphenylene film is obtained. The reaction is extended to a polyvinylchloride (PVC) surface. The mechanism proposed for the formation of this film involves the formation of an aryl radical that reacts with the surface and then with the first grafted aryl group. The film is characterized by infrared reflection absorption spectroscopy (IRRAS), X-ray photoelectron spectroscopy (XPS), water contact angles, and ellipsometry.
- Bouriga, Meriem,Chehimi, Mohamed M.,Combellas, Catherine,Decorse, Philippe,Kanoufi, Frederic,Deronzier, Alain,Pinson, Jean
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- Synthesis and?evaluation of?cytotoxic activity of?arylfurans
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A series of 2-aryl and 2,5-diarylfurans were synthesized and evaluated for their in vitro cytotoxicity against human cancer cells lines and on the proliferation of human peripheral blood mononuclear cells (PBMC) stimulated with phytohemaglutinin (PHA). Three compounds were found to present significant activity against the cancer cell lines without affecting the lymphocyte proliferation in PBMCs, indicating low toxicity to normal cells.
- de Oliveira, Renata B.,de Souza-Fagundes, Elaine M.,Siqueira, Helen A.J.,Leite, Rodrigo S.,Donnici, Claudio L.,Zani, Carlos L.
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p. 756 - 760
(2007/10/03)
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- Pd-EDTA as an efficient catalyst for Suzuki-Miyaura reactions in water
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PdCl2-EDTA complex 1 is an efficient catalyst for the Suzuki-Miyaura reactions of aryl and heteroaryl halides with aryl(heteroaryl)boronic acids in water at 20-100°C. Aryl iodides and bromides undergo the cross-coupling with turnover numbers (T
- Korolev, Dmitrii N.,Bumagin, Nikolay A.
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p. 5751 - 5754
(2007/10/03)
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- New carboxamide compounds having melanin concentrating hormone antagonistic activity, pharmaceutical preparations comprising these compounds and process for their manufacture
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The present invention relates to carboxamide compounds of general formula I wherein the groups and residues A, B, W, X, Y, Z, R1, R2, R3 and k have the meanings given in claim 1. Moreover the invention relates to process for preparing the above mentioned carboxamides as well as pharmaceutical compositions containing at least one carboxamide according to the invention. In view of their MCH-receptor antagonistic activity the pharmaceutical compositions according to the invention are suitable for the treatment of metabolic disorders and/or eating disorders, particularly obesity, bulimia, anorexia, hyperphagia and diabetes.
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Page/Page column 82-83
(2010/02/09)
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- Benzamide nitriles
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Compounds of the formula (I) wherein m, n, A, R1, R2, R3, R4, R5 and R6 are as described herein, together with methods for making the compounds and using the compounds for treatment of diseases or conditions mediated by Cathepsin K.
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- Inhibitors of glycogen synthase kinase 3
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New pyrimidine or pyridine based compounds, compositions and methods of inhibiting the activity of glycogen synthase kinase (GSK3) in vitro and of treatment of GSK3 mediated disorders in vivo are provided. The methods, compounds and compositions of the invention may be employed alone, or in combination with other pharmacologically active agents in the treatment of disorders mediated by GSK3 activity, such as diabetes, Alzheimer's disease and other neurodegenerative disorders, obesity, atherosclerotic cardiovascular disease, essential hypertension, polycystic ovary syndrome, syndrome X, ischemia, traumatic brain injury, bipolar disorder, immunodeficiency or cancer.
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- Inhibitors of glycogen synthase kinase 3
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Novel pyridine and pyrimidine derivatives which selectively inhibit glycogen synthase kinase 3 are provided and methods of preparing these compounds are provided. These compounds are useful in treating certain conditions which may be mediated by glycogen synthase kinase 3.
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- The stille cross coupling reactions on solid support. Link to solution phase directed ortho metalation. An ester linker approach to styryl, biaryl and heterobiaryl carboxylic acids
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The synthesis of the titled compounds by Stille cross coupling on Merrifield resin - linked halo benzoates with stannanes followed by LiOH hydrolysis is reported.
- Chamoin, Sylvie,Houldsworth, Stephen,Snieckus, Victor
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p. 4175 - 4178
(2007/10/03)
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- Efficient palladium-catalyzed synthesis of unsymmetrical donor-acceptor biaryls and polyaryls
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4,4'-Unsymmetrically substituted biphenyls can be synthesized by cross-coupling reactions of substituted aromatic organometallic reagents and aromatic halides catalyzed by palladium complexes.This two-step method from commercially available aromatic halides has been used for the synthesis of a series of donor/acceptor para-substituted biphenyls, D-C6H4-C6H4-A, where D is an electron donor group and A an electron acceptor group, which are of interst as liquid crystal precursors and as having potential in non-linear optics.Biaryls in which the donor-phenyl moiety is replaced by a 2-furyl or 2-thienyl can be synthesized similarly.The method can also be used for the convergent synthesis of previously unreported unsymmetrically substituted polyparaphenylenes D-(C6H4)n-A (n = 3, 4).
- Amatore, Christian,Jutand, Anny,Negri, Serge,Fauvarque, Jean-Francois
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p. 389 - 398
(2007/10/02)
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