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The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD.

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Piperidine – Wikipedia,
Piperidine | C5H109N – PubChem

 

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We have identified and synthesized a series of thiophene containing inhibitors of kinesin spindle protein. SAR studies led to the synthesis of 33, which was co-crystallized with KSP and determined to bind to an allosteric pocket previously described for other known KSP inhibitors.

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In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum.In a patent, 50717-82-3, name is Piperidin-3-one, introducing its new discovery. Recommanded Product: 50717-82-3

The bicyclic 5-isoxazolol zwitterions 4,5,6,7-tetrahydroisoxazolo<4,3-c>pyridin-3-ol (3, iso-THPO), 5,6,7,8-tetrahydro-4H-isoxazolo<4,3-c>azepin-3-ol (12, iso-THAO), and 5,6,7,8-tetrahydro-4H-isoxazolo<3,4-c>azepin-3-ol (13, iso-THIA), which are structurally related to the glycine antagonist 5,6,7,8-tetrahydro-4H-isoxazolo<3,4-d>azepin-3-ol (iso-THAZ), have been synthesized and tested biologically.All of these compounds were glycine antagonists approximetely equipotent with iso-THAZ during microelectrophoretic ejection near cat spinal neurons.In contrast to iso-THAZ, which also interacts with 4-aminobutyric acid (GABA) receptors in rat brains, neither 12 or 13 show any significant affinities for GABA binding or uptake mechanisms in vitro.The glycine antagonist 3 was, however, shown also to be a moderately potent inhibitor of GABA uptake.The structure of 12 was established by an X-ray analysis.The bond lengths of the 5-isoxazolol anionic moiety of 12 are in agreement with a pronounced delocalization of the negative charge of this compound.

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Diacetyl (2,3-butanedione) is an important metabolic marker of several cancers, as well as an important off-flavour component produced during fermentation. As a small molecule in a complex mixture with many other analytes, existing methods for identification and quantitation of diacetyl invariably involves a chromatographic separation step followed by signal integration with an appropriate stoichiometric detector. Here we demonstrate that the chemical reaction of diacetyl with a 1,2-phenylenediamine derivative yields a chemical adduct, 1,4-quinoxaline which can be conjugated on BSA. The BSA-diacetyl adduct can be used to select an adduct-specific monoclonal antibody in a Fab-format from a 45-billion member phage-display library. The availability of this antibody allowed the development of an enzyme-linked immunosorbent assay for diacetyl, based on the 1,4-quinoxaline competition for the antibodies with the diacetyl adduct immobilized on the plate. The described ELISA assay can detect the captured diacetyl in micromolar concentrations, both in water samples and in cell culture medium.

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2-Hydroxy-8-(or 9-)aza-1-oxaspiro[5.5]undec-3-en-5-ones derived from their corresponding 2-furfuryl alcohols were used as key intermediates for the convenient synthesis of several novel 8- and 9-aza-1-oxaspiro[5.5]undecane derivatives.

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Application of 1722-95-8, Because a catalyst decreases the height of the energy barrier, its presence increases the reaction rates of both the forward and the reverse reactions by the same amount.1722-95-8, Name is (R)-2-Methylpiperidine, molecular formula is C6H13N. In a article,once mentioned of 1722-95-8

A series of 2-aryl tryptamines have been identified as high-affinity h5-HT(2A) antagonists. Structure-activity relationship studies have shown that h5-HT(2A) affinity can be attained via modifications to the tryptamine side chain and that selectivity over h5-HT(2C) and hD2 receptors can be controlled by suitable C-2 aryl groups. (C) 2000 Elsevier Science Ltd.

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Piperidine – Wikipedia,
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Traceless solid-phase synthesis represents an ultimate sophisticated synthetic strategy on insoluble supports. Compounds synthesized on solid supports can be released without a trace of the linker that was used to tether the intermediates during the synthesis. Thus, the target products are composed only of the components (atoms, functional groups) inherent to the target core structure. A wide variety of synthetic strategies have been developed to prepare products in a traceless manner, and this review is dedicated to all aspects of traceless solid-phase organic synthesis. Importantly, the synthesis does not need to be carried out on a linker designed for traceless synthesis; most of the synthetic approaches described herein were developed using standard, commercially available linkers (originally devised for solid-phase peptide synthesis). The type of structure prepared in a traceless fashion is not restricted. The individual synthetic approaches are divided into eight sections, each devoted to a different methodology for traceless synthesis. Each section consists of a brief outline of the synthetic strategy followed by a description of individual reported syntheses.

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Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 41661-47-6, molcular formula is C5H9NO, introducing its new discovery. name: 4-Piperidinone

A novel compound represented by the formula (I): wherein rings A and B each represents an optionally substituted aromatic ring, or rings A and B may be bonded to each other through linking between bonds or substituents thereof to form a ring; ring C represents a nitrogenous saturated heterocycle optionally having one or more substituents besides the oxo (provided that 2,3-dioxopyrrolidine ring is excluded); R1 represents hydrogen, an optionally substituted hydrocarbon group, or an optionally substituted heterocyclic group; and——– indicates a single bond or a double bond. It has high antagonistic activity against a tachykinin receptor, especially an SP receptor.

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The invention discloses a biologically active tetrahydroimidazo thiazole and pyridine hydrochloride salt compound and its preparation method, which belongs to the technical field of drug synthesis. Technical proposal of the invention points are: with the biological activity of the tetrahydro-benzothiazole and pyridine hydrochloride salt compound, has the following structure: , Wherein R is cyano phenyl, tert-butyl, phenyl, trifluoromethyl, chlorophenyl or among methoxyphenyl. The invention also discloses the has biological activity tetrahydro-benzothiazole and pyridine salt to the acid salt of the compound of preparation method. The invention a new method to synthesize a series of biologically active tetrahydroimidazo thiazole and pyridine salt to the acid salt of the compound, the reaction process is simple and easy operation, the raw material is cheap, relatively high reaction efficiency and good repeatability, biological active effect is obvious. (by machine translation)

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In the present study, a series of mono-carbonyl analogues of curcumin were designed and synthesized by deleting the reactive beta-diketone moiety, which is responsible for the pharmacokinetic limitation of curcumin. We demonstrated that 4 of 9 curcumin analogues were selective inhibitors of human and rodent 11beta-HSD1. The level of this inhibitor was 4-20 times more than that of curcumin. Curcumin analogues weakly inhibited 11beta-HSD2, and further analyses revealed that these compounds were highly selective, favoring 11beta-HSD1. These 4 curcumin analogues are potential therapeutic agents for type-2 diabetes by targeting 11beta-HSD1. The compound 8 displays anti-diabetic properties in diabetic mice induced by streptozocin and high-fat-diet (STZHFD).

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