cas 90035-34-0, 4'-TRIFLUOROMETHYL-BIPHENYL-4-CARBALDEHYDE

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The Discovery of Novel ACA Derivatives as Specific TRPM2 Inhibitors that Reduce Ischemic Injury Both in Vitro and in Vivo
The transient receptor potential melastatin 2 (TRPM2) channel is associated with ischemia/reperfusion injury, inflammation, cancer, and neurodegenerative diseases. However, the limit of specific inhibitors impedes the development of TRPM2-targeted therapeutic agents. To discover more potent and selective TRPM2 inhibitors, 59 N-(p-amylcinnamoyl) anthranilic acid (ACA) derivatives were synthesized and evaluated using calcium imaging and electrophysiology approaches. Systematic structure-activity relationship studies resulted in some potent compounds inhibiting the TRPM2 channel with sub-micromolar half-maximal inhibitory concentration values. Among them, the preferred compound A23 exhibited TRPM2 selectivity over TRPM8 and TRPV1 channels as well as phospholipase A2 and showed neuroprotective activity in vitro. Following pharmacokinetic studies, A23 was further evaluated in a transient middle cerebral artery occlusion model in vivo, which significantly reduced cerebral infarction. These data indicate that A23 might serve as a useful tool for TRPM2-related research as well as a lead compound for the development of therapeutic agents for ischemic injury.
Zhang, Han,Yu, Peilin,Lin, Hongwei,Jin, Zefang,Zhao, Siqi,Zhang, Yi,Xu, Qingxia,Jin, Hongwei,Liu, Zhenming,Yang, Wei,Zhang, Liangren
p. 3976 - 3996
(2021/05/04)

KDS2010, a Newly Developed Reversible MAO-B Inhibitor, as an Effective Therapeutic Candidate for Parkinson’s Disease
Monoamine oxidase-B (MAO-B) is a well-established therapeutic target for Parkinson’s disease (PD); however, previous clinical studies on currently available irreversible MAO-B inhibitors have yielded disappointing neuroprotective effects. Here, we tested the therapeutic potential of KDS2010, a recently synthesized potent, selective, and reversible MAO-B inhibitor in multiple animal models of PD. We designed and synthesized a series of α-aminoamide derivatives and found that derivative KDS2010 exhibited the highest potency, specificity, reversibility, and bioavailability (> 100%). In addition, KDS2010 demonstrated significant neuroprotective and anti-neuroinflammatory efficacy against nigrostriatal pathway destruction in the mouse MPTP model of parkinsonism. Treatment with KDS2010 also alleviated parkinsonian motor dysfunction in 6-hydroxydopamine-induced and A53T mutant α-synuclein overexpression rat models of PD. Moreover, KDS2010 showed virtually no toxicity or side effects in non-human primates. KDS2010 could be a next-generation therapeutic candidate for PD.
Nam, Min-Ho,Park, Jong-Hyun,Song, Hyo Jung,Choi, Ji Won,Kim, Siwon,Jang, Bo Ko,Yoon, Hyung Ho,Heo, Jun Young,Lee, Hyowon,An, Heeyoung,Kim, Hyeon Jeong,Park, Sun Jun,Cho, Doo-Wan,Yang, Young-Su,Han, Su-Cheol,Kim, Sangwook,Oh, Soo-Jin,Jeon, Sang Ryong,Park, Ki Duk,Lee, C. Justin
p. 1729 - 1747
(2021/10/08)

Oxazolidinone compound as well as preparation method, application and pharmaceutical composition thereof
The invention relates to an oxazolidinone compound used as an Lp-PLA2 covalent inhibitor and a pharmaceutical composition of the oxazolidinone compound, the structure of the oxazolidinone compound isshown as a general formula I, and R1, R2 and R3 are defined as the specification and claims. The compound shown in the general formula I or the stereoisomer or the pharmaceutically acceptable salt thereof can be used as the Lp-PLA2 covalent inhibitor to prevent and/or treat and/or improve diseases related to Lp-PLA2 enzyme activity. Meanwhile, the stereoisomer or the pharmaceutically acceptable salt of the compound shown in the general formula I can be used as an Lp-PLA2 specific molecular probe.
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Paragraph 0108-0110

(2020/11/05)

Monosubstituted, Anionic Imidazolyl Ligands from N?H NHC Precursors and Their Activity in Pd-Catalyzed Cross-Coupling Reactions
We report that treatment of several 2-diphenylphosphinoimidazoles with Pd(II) salts generates monosubstituted N?H NHC?Pd complexes via insertion into the C?P bond. Removal of the N?H proton in situ leads to anionic (X-type) or imidazolyl-Pd complexes that are highly stable and catalytically active, achieving up to 340,000 turnovers at 1 ppm catalyst loading in Suzuki-Miyaura reactions. DFT-calculated Tolman electronic parameters for the sterically small ligands suggest that these ligands are significantly more donating than traditional NHCs, which provides a rationale for rapid cross-coupling catalysis. Excellent reactivity is also demonstrated in Sonogashira reactions. (Figure presented.).
Clark, Kyle J.,Ess, Daniel H.,Jensen, Christopher A.,Kenney, Karissa C.,Larson, Alexandra J. S.,Martinez, Erin E.,Michaelis, David J.,Nazari, S. Hadi,Smith, Stacey J.,Valdivia-Berroeta, Gabriel A.
supporting information

(2020/07/06)

Method for synthesizing biphenyl compound by taking phenol as raw material
The invention discloses a method for synthesizing a biphenyl compound by using phenol as a raw material in the technical field of organic chemical synthesis, which comprises the following steps: carrying out a mixed reaction process on phenol or substituted phenol, alkali and 50-90% ethanol aqueous solution, slowly introducing sulfonyl fluoride gas, and carrying out magnetic stirring reaction at normal temperature for 4-12 hours, adding arylboronic acid, alkali and a palladium catalyst into a round-bottom flask, continuing to react for 6-12 hours at normal temperature, after the reaction is finished, adding a saturated edible salt solution into the round-bottom flask, carrying out a water quenching reaction process to obtain a reaction mixture, extracting a reaction product from the reaction mixture by using ethyl acetate, combining organic phases, concentrating filtrate, and separating the concentrated filtrate by using column chromatography to obtain analytically pure biphenyl or terphenyl compounds. By using the method, on one hand, the production cost of the biphenyl compound is reduced, and on the other hand, the method also has a wide application prospect in the aspects of synthesis of natural products, medicines, pesticides, herbicides, polymer conduction materials, liquid crystal materials and the like.
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Paragraph 0044-0046

(2020/07/15)

(N-Heterocyclic carbene) ion-pair palladium complexes: Suzuki–Miyaura cross-coupling studies in neat water under mild conditions
The synthesis and characterization of a series of (N-heterocyclic carbene)PdCl3?(NMe3H)+ ion-pair complexes are presented. Applying the quaternary ammonium salt as the function with NHC–Pd(II) complexes yields the new ion-pair complexes. The NHC–Pd(II) ion-pair complexes work well by undergoing the Suzuki–Miyaura reaction with aryl chloride substrates in water under mild conditions in air at room temperature. Twenty products resulting from Suzuki–Miyaura coupling reactions carried out in the presence of the new NHC–Pd(II) ion-pair complex under mild optimal conditions were examined to determine the optimum yields.
Chen, Ming-Tsz,Lin, Yu-Hsuan,Jian, Kun-Han
(2020/08/05)

RADIOLABELED DARAPLADIB AND ANALOGS THEREOF AND THEIR USE AS IMAGING COMPOUNDS
The present inventors have developed new radiolabeled Darapladib and analogs thereof which can be used for the specific detection of vulnerable atherosclerotic plaques by targeting lipoprotein-associated phospholipase A2 (Lp-PLA2) which is a biomarker of
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Page/Page column 33

(2019/04/26)

Regioselectivity of thiouracil alkylation: Application to optimization of Darapladib synthesis
Darapladib is one of the most potent Lp-PLA2 (Lipoprotein-associated phospholipase A2) inhibitor with an IC50 of 0.25 nM. We demonstrate that a crucial step of Darapladib synthesis was not correctly described in the litera
Guibbal, Florian,Bénard, Sébastien,Patché, Jessica,Meneyrol, Vincent,Couprie, Jo?l,Yong-Sang, Jennyfer,Meilhac, Olivier,Jestin, Emmanuelle
supporting information
p. 787 - 792
(2018/01/17)

Novel π-conjugated molecules based on diimidazopyridine: Significantly improved the photophysical, thermal and electrochemical properties bearing different aryl substituents
A series of π-conjugated molecules based on diimidazolepyridine derivatives were designed, synthesized by Suzuki coupling reaction and cyclization reaction and characterized. Diimidazolepyridine motif as the main structure could improve the thermal stabil
Huang, Xin,Tian, Jinchang,Xu, Feng,Liu, Xiaochong,Li, Yuqin,Guo, Yanyan,Chu, Wenyi,Sun, Zhizhong
supporting information
p. 681 - 686
(2018/01/16)

Aromatic diamine and preparation method thereof
The invention relates to aromatic diamine and a preparation method thereof. The structure of the aromatic diamine is as shown in the following formula I, wherein R1 and R2 are independently selected from the group: H atoms, CnH2nCF3 or -C6H5, and n is an integer of 0-10. The aromatic diamine synthesis route is simple, raw materials are relatively cheap and can be easily obtained, and the preparedpolyimide film has good optical transmission and high solubility.
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Paragraph 0116; 0117; 0118; 0119

(2018/09/21)

Carboxylic acid derivatives and preparation method and use in medicines thereof
The invention relates to carboxylic acid derivatives and a preparation method and use in medicines thereof. Specifically, the invention relates to carboxylic acid derivatives as shown in the general formula (I), a preparation method and pharmaceutically a
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Paragraph 0147; 0152; 0153-0155

(2018/03/24)

One-Pot Tandem Photoredox and Cross-Coupling Catalysis with a Single Palladium Carbodicarbene Complex
The combination of conventional transition-metal-catalyzed coupling (2 e? process) and photoredox catalysis (1 e? process) has emerged as a powerful approach to catalyze difficult cross-coupling reactions under mild reaction conditions. Reported is a palladium carbodicarbene (CDC) complex that mediates both a Suzuki–Miyaura coupling and photoredox catalysis for C?N bond formation upon visible-light irradiation. These two catalytic pathways can be combined to promote both conventional transition-metal-catalyzed coupling and photoredox catalysis to mediate C?H arylation under ambient conditions with a single catalyst in an efficient one-pot process.
Hsu, Yu-Cheng,Wang, Vincent C.-C.,Au-Yeung, Ka-Chun,Tsai, Chung-Yu,Chang, Chun-Chi,Lin, Bo-Chao,Chan, Yi-Tsu,Hsu, Chao-Ping,Yap, Glenn P. A.,Jurca, Titel,Ong, Tiow-Gan
supporting information
p. 4622 - 4626
(2018/03/21)

Compounds
Pyrimidone compounds of formula (I): are inhibitors of the enzyme Lp-PLA2 and are of use in treating atherosclerosis.
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Page/Page column 14; 22

(2016/05/11)

Probing the Azaaurone Scaffold against the Hepatic and Erythrocytic Stages of Malaria Parasites
The potential of azaaurones as dual-stage antimalarial agents was investigated by assessing the effect of a small library of azaaurones on the inhibition of liver and intraerythrocytic lifecycle stages of the malaria parasite. The whole series was screened against the blood stage of a chloroquine-resistant Plasmodium falciparum strain and the liver stage of P. berghei, yielding compounds with dual-stage activity and sub-micromolar potency against erythrocytic parasites. Studies with genetically modified parasites, using a phenotypic assay based on the P. falciparum Dd2-ScDHODH line, which expresses yeast dihydroorotate dehydrogenase (DHODH), showed that one of the azaaurone derivatives has the potential to inhibit the parasite mitochondrial electron-transport chain. The global urgency in finding new therapies for malaria, especially against the underexplored liver stage, associated with chemical tractability of azaaurones, warrants further development of this chemotype. Overall, these results emphasize the azaaurone chemotype as a promising scaffold for dual-stage antimalarials.
Carrasco, Marta P.,Machado, Marta,Gon?alves, Lídia,Sharma, Moni,Gut, Jiri,Lukens, Amanda K.,Wirth, Dyann F.,André, Vania,Duarte, Maria Teresa,Guedes, Rita C.,dos Santos, Daniel J. V. A.,Rosenthal, Philip J.,Mazitschek, Ralph,Prudêncio, Miguel,Moreira, Rui
supporting information
p. 2194 - 2204
(2016/10/19)

VP1 crystal structure-guided exploration and optimization of 4,5-dimethoxybenzene-based inhibitors of rhinovirus 14 infection
Human rhinoviruses (HRV) are the predominant cause of common colds and flu-like illnesses, but are also responsible for virus-induced exacerbations of asthma and chronic obstructive pulmonary disease. However, to date, no drug has been approved yet for clinical use. In this study, we present the results of the structure-based lead optimization of a class of new small-molecule inhibitors that we previously reported to bind into the pocket beneath the canyon of the VP1 protein. A small series of analogues that we designed based on the available structure and interaction data were synthesized and evaluated for their potency to inhibit the replication of HRV serotype 14. 2-(4,5-Dimethoxy-2-nitrophenyl)-1-(4-(pyridin-4-yl)phenyl)ethanol (3v) was found to be a potent inhibitor exhibiting micromolar activity (EC50 Combining double low line 3.4 ± 1.0 μM) with a toxicity for HeLa cells that was significantly lower than that of our previous hit (LPCRW-0005, CC50 Combining double low line 104.0 ± 22.2 μM; 3v, CC50 > 263 μM).
Da Costa, Laurène,Roche, Manon,Scheers, Els,Coluccia, Antonio,Neyts, Johan,Terme, Thierry,Leyssen, Pieter,Silvestri, Romano,Vanelle, Patrice
p. 453 - 462
(2016/04/19)

Synthesis of Biaryls through Nickel-Catalyzed Suzuki-Miyaura Coupling of Amides by Carbon-Nitrogen Bond Cleavage
The first Ni-catalyzed Suzuki-Miyaura coupling of amides for the synthesis of widely occurring biaryl compounds through N-C amide bond activation is reported. The reaction tolerates a wide range of electron-withdrawing, electron-neutral, and electron-donating substituents on both coupling partners. The reaction constitutes the first example of the Ni-catalyzed generation of aryl electrophiles from bench-stable amides with potential applications for a broad range of organometallic reactions. Breaking and making: The first nickel-catalyzed Suzuki-Miyaura coupling of amides for the synthesis of biaryl compounds through N-C amide bond cleavage is reported. The reaction tolerates a wide range of sensitive and electronically diverse substituents on both coupling partners.
Shi, Shicheng,Meng, Guangrong,Szostak, Michal
p. 6959 - 6963
(2016/06/13)

Efficient symmetrical bidentate dioxime ligand-accelerated homogeneous palladium-catalyzed Suzuki-Miyaura coupling reactions of aryl chlorides
A series of N,O-bidentate ligands were synthesized using the Vilsmeier-Haack reaction and oximation. 2,5-Dihydroxyterephthalaldehyde dioxime (L8) as an efficient N,O-symmetrical bidentate ligand was prepared from hydroquinone. It was studied as a high activity ligand for palladium-catalyzed Suzuki-Miyaura cross-coupling reactions of aryl chlorides with arylboronic acids under mild conditions. The coupling reactions were performed in the presence of PdCl2 as the catalyst, L8 as the ligand, Na2CO3 as the base, PEG-400 as the PTC and in ethanol/water (1?:?1) as an environmentally benign solvent at 85 °C. Plentiful biaryls were obtained by the optimized reaction with good yields at a low palladium loading of 0.20 mol%.
Song, Jinyi,Zhao, Hongyan,Liu, Yang,Han, Huatao,Li, Zhuofei,Chu, Wenyi,Sun, Zhizhong
p. 372 - 376
(2016/12/30)

Mn-salen catalysed benzylic C-H activation for the synthesis of aryl [18F]CF3-containing PET probes
The development of a Mn-salen complex catalysed oxidative benzylic fluorination of non-activated C-H bonds using [18F]fluoride is described for installation of [18F]CHRF, [18F]CR2F and particularly [18/sup
Carroll,Evans,Spivey,Aboagye
supporting information
p. 8439 - 8441
(2015/05/20)

PARTIALLY SATURATED NITROGEN-CONTAINING HETEROCYCLIC COMPOUND
There are provided compounds having a superior PHD2 inhibitory effect that are represented by general formula (I'): (in the above-mentioned general formula (I'), W, Y, R2, R3, R4, and Y4 are as described hereinabove), or pharmaceutically acceptable salts thereof.
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Paragraph 0295; 0296

(2015/06/17)

A novel 4-aminoantipyrine-Pd(II) complex catalyzes Suzuki-Miyaura cross-coupling reactions of aryl halides
A simple and efficient catalytic system based on a Pd complex of 4-aminoantipyrine, 4-AAP-Pd(II), was found to be highly active for Suzuki-Miyaura cross-coupling of aryl iodides and bromides with phenylboronic acids under mild reaction conditions. Good to excellent product yields from the cross-coupling reaction can be achieved when the reaction is carried out in ethanol, in the open air, using low loading of 4-AAP-Pd(II) as a precatalyst, and in the presence of aqueous K2CO3 as the base. A variety of functional groups are tolerated.
Contreras-Celedn, Claudia A.,Mendoza-Rayo, Daro,Rincn-Medina, Jos A.,Chacn-Garca, Luis
supporting information
p. 2821 - 2826
(2015/02/19)

Nickel-catalysed Suzuki-Miyaura cross-coupling reactions of aryl halides with arylboronic acids in ionic liquids
An efficient strategy for the nickel-catalysed synthesis of biaryls and terphenyls has been developed in environmentally-friendly reaction media. In the presence of β-diketone and PPh3 ligands, Ni(TFA)2 acted as an effective catalyst for the Suzuki-Miyaura cross-coupling of aryl halides and arylboronic acids in an ionic liquid solution. Biaryls and terphenyls were obtained in good yields under this catalytic system.
Wang, Man,Yuan, Xiaobin,Li, Hongyu,Ren, Limin,Sun, Zhizhong,Hou, Yanjun,Chu, Wenyi
supporting information
p. 154 - 157
(2015/02/19)

AZOLE HETEROCYCLIC COMPOUND, PREPARATION METHOD, PHARMACEUTICAL COMPOSITION AND USE
The present invention relates to the filed of pharmarcutical chemistry, and in particular, to a novel class of azole compounds represented by general formula (I), (II) or (III) amd a preparation method thereof, a pharmarcutical composition with the compounds as active components, and a use of the azole compounds and the pharmarcutical composition in the preparation of a medicament for treatment of diseases associated with Lp-PLA2 enzyme activities, wherein each substituent is as deinfed in the specifictaion.
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Paragraph 0125; 0126

(2014/05/20)

AZOLE HETEROCYCLIC COMPOUND, PREPARATION METHOD, PHARMACEUTICAL COMPOSITION AND USE
The present invention relates to the field of pharmaceutical chemistry, and in particular, to a novel class of azole compounds represented by general formula (I), (II) or (III) and a preparation method thereof, a pharmaceutical composition with the compounds as active components, and a use of the azole compounds and the pharmaceutical composition in the preparation of a medicament for treatment of diseases associated with Lp-PLA2 enzyme activities, wherein each substituent is as defined in the specification.
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Paragraph 0471; 0472

(2014/06/25)

Discovery and structure-activity relationships of pyrrolone antimalarials
In the pursuit of new antimalarial leads, a phenotypic screening of various commercially sourced compound libraries was undertaken by the World Health Organisation Programme for Research and Training in Tropical Diseases (WHO-TDR). We report here the detailed characterization of one of the hits from this process, TDR32750 (8a), which showed potent activity against Plasmodium falciparum K1 (EC50 ～ 9 nM), good selectivity (>2000-fold) compared to a mammalian cell line (L6), and significant activity against a rodent model of malaria when administered intraperitoneally. Structure-activity relationship studies have indicated ways in which the molecule could be optimized. This compound represents an exciting start point for a drug discovery program for the development of a novel antimalarial.
Murugesan, Dinakaran,Mital, Alka,Kaiser, Marcel,Shackleford, David M.,Morizzi, Julia,Katneni, Kasiram,Campbell, Michael,Hudson, Alan,Charman, Susan A.,Yeates, Clive,Gilbert, Ian H.
supporting information
p. 2975 - 2990
(2013/05/23)

COMPOUNDS
Disclosed are compounds that inhibit Lp-PLA2 activity, processes for their preparation, compositions containing them and their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease, and/or diabetic macular edema.
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Page/Page column 41

(2012/06/30)

Glucagon Receptor Modulators
The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, A1, A2, A3, A4, L, B1, B2, B3 and B4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.
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Page/Page column 15

(2012/07/13)

18-Crown-6 promoting Pd/C-catalyzed cross-coupling reaction of aryl bromides and arylboronic acids in aqueous media
Pd/C-catalyzed Suzuki-Miyaura cross-coupling between aryl bromides and arylboronic acids in 50% methanol aqueous solution proceeded smoothly in the presence of 18-crown-6. Various aryl bromides bearing electron-withdrawing groups and electron-donating gro
Chu, Wenyi,Li, Xinmin,Hou, Yanjun,Wang, Hua,Li, Hongyu,Yuan, Xiaobin,Sun, Zhizhong
p. 478 - 482
(2012/10/29)

PEPTIDASE INHIBITORS
Novel compounds of the formula (I) wherein R1, R2, D, A, B and X have the meanings defined herein, pharmaceutical compositions comprising them as active ingredient, as well as their use in medicine, in particular as peptidase inhibitors, more specifically
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Page/Page column 113

(2012/10/18)

Efficient screening and library generation in parallel C-C coupling reactions mediated by Organosilica SiliaCat palladium catalysts
Organosilica SiliaCat palladium catalysts applied to the conversion of widely different substrates in Suzuki, Sonogashira, and Heck coupling reactions run in a parallel synthesizer enable quick screening of the reaction system with identification of the best reaction conditions and rapid library generation.
Pandarus, Valerica,Gingras, Genevieve,Beland, Francois,Ciriminna, Rosaria,Pagliaro, Mario
scheme or table
p. 117 - 122
(2012/06/01)

An efficient protocol for the palladium-catalysed Suzuki-Miyaura cross-coupling
The palladacyclic catalyst precursor received by ortho-palladation of ([1,1′-biphenyl]-2-yloxy)diisopropyl-phosphine represents a highly active system for Suzuki-Miyaura cross-coupling reactions when used in neat water. An efficient, broadly applicable and sustainable aqueous protocol was developed using 2.5 eq. of Na2CO3 as base, allowing the reaction to be performed under air and at ambient temperature with Pd loadings of 0.04 mol%. Coupling products are obtained in high yields and excellent purity by simple filtration with no organic solvents needed throughout the whole reaction. A broad variety of functional groups are tolerated and a large number of substrates can be applied with this protocol. The crystal structure of the palladacyclic catalyst precursor is presented as well as investigations targeting the nature of catalyst activation and the active catalytic species.
Marziale, Alexander N.,Jantke, Dominik,Faul, Stefan H.,Reiner, Thomas,Herdtweck, Eberhardt,Eppinger, Joerg
supporting information; experimental part
p. 169 - 177
(2011/03/23)

Nickel-catalyzed cross-coupling of organogold reagents
Organogold compounds undergo nickel-catalyzed cross-coupling reactions with aryl and vinyl bromides in high yield under mild conditions. The reaction tolerates both electron-rich and electron-poor organogold complexes, and olefinic bromides undergo cross-coupling with high stereoselectivity. This novel transformation links well-established nickel catalysis with more recent developments in organogold transformations.
Hirner, Joshua J.,Blum, Suzanne A.
scheme or table
p. 1299 - 1302
(2011/04/22)

Shear- and UV-induced fluorescence switching in stilbenic ?-dimer crystals powered by reversible [2 + 2] cycloaddition
We have designed and synthesized asymmetric cyano-stilbene derivatives containing trifluoromethyl (-CF3) substituents with the aim ofproducing tightly packed ?-dimer systems that as crystals exhibit re versible [2 + 2] cycloaddition with charac
Chung, Jong Won,You, Youngmin,Hoh, Hyun Sue,An, Byeong-Kwan,Yoon, Seong-Jun,et al.
supporting information; experimental part
p. 8163 - 8172
(2009/12/02)

BENZOAZEPIN-OXY-ACETIC ACID DERIVATIVES AS PPAR-DELTA AGONISTS USED FOR THE INCREASE OF HDL-C, LOWER LDL-C AND LOWER CHOLESTEROL
The invention is directed to compounds of Formula (I) useful as PPAR agonists. Pharmaceutical compositions and methods of treating one or more conditions including, but not limited to, diabetes, nephropathy, neuropathy, retinopathy, polycystic ovary syndr
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Page/Page column 79

(2008/06/13)

3-BENZYLTHIO-1,2,4-TRIAZINE-5 (2H)-ONE AS PAF-AH INHIBITORS
The invention relates to 3-benzylthio-1,2,4-triazine-5 (2H)-one of formula I, methods for the production thereof, and the use thereof for producing medicaments that are used for the treatment and/or prevention of diseases, especially chronic inflammatory diseases, such as diseases of the rheumatic type, and cardiovascular diseases, e.g. dyslipidemia, arteriosclerosis, and coronary heart diseases.
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Page/Page column 27

(2010/11/08)

SUBSTITUTED 1,2,4-TRIAZIN-5(2H)-ONES
The invention relates to substituted 1,2,4-triazin-5(2H)-ones, to a method for the production thereof, and to their use for producing medicaments for treating and/or preventing diseases, particularly chronic inflammatory diseases, for example, rheumatoid
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Page/Page column 30

(2010/11/08)

3-CYCLOALKYL-1,2,4-TRIAZIN-5(2H)-ONES
The invention relates to 3-cycloalkyl-1,2,4-triazin-5(2H)-ones, to a method for the production thereof, and to their use for producing medicaments for treating and/or preventing diseases, particularly chronic inflammatory diseases, for example, rheumatoid
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Page/Page column 24

(2010/11/08)

AMIDE-SUBSTITUTED 1,2,4-TRIAZIN-5(2H)-ONES FOR THE TREATMENT OF CHRONICALLY INFLAMMATORY DISEASES
The invention relates to amide-substituted 1,2,4-triazin-5(2H)-ones, to methods for the production thereof, and to the use of the same for producing medicaments for the treatment and/or prophylaxis of diseases, especially chronically inflammatory diseases such as rheumatoid diseases, and cardiovascular diseases such as dyslipidemia, arteriosclerosis and coronary heart diseases Formula (I).
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Page/Page column 34

(2010/02/10)

NOVEL DERIVATIVES OF DICARBOXYLIC ACID HAVING PHARMACEUTICAL PROPERTIES
The invention relates to compounds of formulae (II), (IV), and (VI) as shown below, wherein the several variable groups are as defined in the specification and claims. Processes for making these materials, and methods for using them in the synthesis of compounds for treatment of cardiovascular disorders and fibrotic disorders are also disclosed.
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Page/Page column 43

(2008/06/13)

GLUCAGON RECEPTOR ANTAGONISTS, PREPARATION AND THERAPEUTIC USES
The present invention discloses novel compounds of Formula (I), or pharmaceutically acceptable salts thereof, which have glucagon receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of using them to treat diabetic and other glucagon related metabolic disorders, and the like.
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Page/Page column 43; 55-56

(2010/02/15)

Pyrimidinone compounds
Pyrimidinone compounds of formula (I) are inhibitors of the enzyme Lp-PLA2 and of use in therapy, in particular for treating atherosclerosis.
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Page/Page column 11

(2008/06/13)

A convenient microwave assisted arylzinc generation-Negishi coupling protocol
Arylzinc reagents were readily prepared from aryl iodides using a Zn-Cu couple in a microwave environment. A sequential arylzinc formation-Negishi cross-coupling protocol suitable for parallel high-throughput synthesis has been developed.
Mutule, Ilga,Suna, Edgars
p. 3909 - 3912
(2007/10/03)

Pyridinone derivatives for treatment of atherosclerosis
Compounds of formula (I): are inhibitors of the enzyme Lp-PLA2 and are of use in therapy, in particular for treating atherosclerosis.
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(2008/06/13)

NOVEL COMPOUNDS
Compounds of formula (I): are inhibitors of the enzyme Lp-PLA2 and are of use in therapy, in particular for treating atherosclerosis. In Formula (I) R1, R2, R3, R4, R5, R6, X and Y are as d
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Page/Page column 18

(2010/02/07)

An easily prepared, air and moisture stable, resin-bound palladium catalyst for Suzuki cross-coupling reactions
An air and moisture stable polymer supported palladium catalyst easily prepared from a commercial available thiourea resin Deloxan THP was found to enable Suzuki cross-coupling reactions to be carried out in high yields and convenient manner.
Zhang, Tony Y.,Allen, Matthew J.
p. 5813 - 5816
(2007/10/03)

Anti-coagulants of the 4-hydroxycoumarin type and rodenticidal compositions (baits) comprising such anti-coagulants
Compounds having blood-anticoagulant properties of the general molecular formula: STR1 in which Z represents a halogen atom, preferably a chlorine atom, and n is 0, 1 or 2 and R4 represents either (1) a grouping which comprises a phenylene radical attached directly or indirectly to the tetralin ring and having in the para position (with respect to such attachment) an electron-withdrawing atom or group whose rotational volume substantially does not exceed that of a phenyl group and which forms together with said phenylene radical a polarizable structure, or (2) a grouping selected from: STR2 or (3) a grouping which comprises a phenylene radical attached directly to the tetralin ring and having in the para position (with respect to such attachment) a substituted furanyl or thiophenyl radical attached thereto directly or through oxygen and/or methylene, said furanyl or thiophenyl radical having such an electron-withdrawing atom or group as a substituent in a position forming with the furanyl or thiophenyl radical a polarizable structure, compounds of the type (1) in which R4 contains two phenylene radicals linked essentially linearly by an aliphatic chain comprising a methylene radical or radicals and optionally at least one oxygen or sulphur atom being preferred. Also included are the processes for the preparation of such compound; rodenticidal compositions containing them; and a method for controlling rodents by applying such a composition.
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(2008/06/13)