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A compound represented by the general formula: (I) (wherein R1 means a 3- to 10-membered nonaromatic heterocyclic group or the like; R2 and R3 mean a hydrogen atom; R4, R5, R6 and R7 are the same or different and mean a hydrogen atom, a halogen atom, a C1-6 alkyl group or the like; R8 means a hydrogen atom or the like; R9 means a 3- to 10-membered nonaromatic heterocyclic group or the like; n means an integer of 1 to 2; and X means a group represented by the formula -CH= or a nitrogen atom), a salt thereof or a hydrate thereof has an excellent hepatocyte growth factor receptor (HGFR) inhibitory action, and exhibits an anti-tumor action, angiogenesis inhibitory action or cancer metastasis inhibitory action.

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The present invention relates to 1 – carbonyl Radix Salviae Miltiorrhizae one IIA derivative and its preparation, and its preparation of cardiovascular disease, cerebrovascular disease, liver and kidney disease, respiratory disease, tumor and the like 1 – carbonyl Radix Salviae Miltiorrhizae one IIA sulfonic acid related to the use of the drug in the target. The present invention provides a 1 – carbonyl Radix Salviae Miltiorrhizae one IIA derivatives of formula (I) is shown. R is selected from: , Wherein R1 Selected from hydrogen, alkyl, heterocyclic alkyl, and alkyl and substituted heterocyclic alkyl can be substituted, substituent is alkyl, alkyl amino alkyl; R2 Selected from hydrogen, alkyl, heterocyclic alkyl, and alkyl and substituted heterocyclic alkyl can be substituted, substituent is alkyl, alkyl amino alkyl. (by machine translation)

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The invention discloses a new formula I shown of the prolyl hydroxylase with the histone deacetylase inhibitor enzyme pair and its preparation method and application, by simultaneously inhibiting prolyl hydroxylase (PHD) and histone deacetylase (HDAC) activity, the role of selectively enhancing the hypoxic induction factor – 2 alpha (HIF – 2 alpha) level, it is expected to become the new radiation protective drug. (by machine translation)

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The invention provides 4-{[1-(aminocarbonyl)-4-piperidinyl]amino}-N-[(3,4-dimethylphenyl)methyl]-1-ethyl-1H-pyrazolo[3,4-b]pyridine-5-carb oxamide, which is the compound of formula (I), or a salt thereof. The invention also provides the use of said compound or a pharmaceutically acceptable salt thereof as an inhibitor of phosphodiesterase type IV (PDE4), for example in the treatment and/or prophylaxis of an inflammatory and/or allergic disease, cognitive impairment or depression in a mammal. In particular, the invention provides the use of the compound or pharmaceutically acceptable salt in the treatment and/or prophylaxis of atopic dermatitis in a mammal, for example by external topical administration to the mammal such as a human. Pharmaceutical compositions containing said compound or salt, in particular suitable for external topical administration, are also provided.

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The present invention relates to compounds comprising the following formula: R0?Q?X?Q??W?U?V?G?M??(I) These compounds are useful as pharmacologically active compounds. They exhibit an antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardiovascular disorders such as thromboembolic diseases or restenoses. These compounds are reversible inhibitors of the blood clotting enzymes factor Xa (FXa) and/or factor VIIa (FVIIa), and can generally be used to treat, prevent, or cure conditions in which an undesired activity of factor Xa and/or factor VIIa is present, or where inhibition of factor Xa and/or factor VIIa is intended. The invention further relates to processes for the preparation of these compounds, methods of their use (e.g., as active ingredients in pharmaceuticals), and pharmaceutical preparations comprising them.

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The incorporation of constrained tertiary amines into an existing class of N-benzyl-4-aminopiperidinyl chromone-based MCHr1 antagonists led to the identification of a series of chiral racemic compounds that displayed good to excellent functional potency, binding affinity, and selectivity over the hERG channel. Further separation of two distinct chiral racemic compounds into their corresponding pairs of enantiomers revealed a considerable selectivity for MCHr1 for one configuration, in addition to a striking difference in oral exposure between one pair of enantiomers in diet-induced obese mice. Oral administration of the most potent compound in this class in the same animal model led to significant reduction of fat mass in a semi-chronic model for weight loss.

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The invention belongs to the technical field of pharmaceutical chemistry, and in particular relates to magnolol series derivatives and its preparation and use. The invention of the magnolol series derivatives is mainly magnolol 5 bit substituted derivatives, magnolol series derivatives as formula I. The invention also provides a series of derivatives of the magnolol preparation method and use thereof. The present invention provides of the magnolol series derivatives through the cell toxicity test proves that the compound has very good anti-tumor activity, in the preparation of a medicament for the treatment of cancer has broad application prospects. (by machine translation)

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Metal-catalyzed cross-coupling reactions are among the most important transformations in organic synthesis. However, the use of C-H activation for sp2 C-N bond formation remains one of the major challenges in the field of cross-coupling chemistry. Described herein is the first example of the synergistic combination of copper catalysis and electrocatalysis for aryl C-H amination under mild reaction conditions in an atom-and step-economical manner with the liberation of H2 as the sole and benign byproduct.

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The invention relates to compounds of the formula 1 and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein R1, R2, R3, and R4 are as defined herein. The invention also relates to methods of treating abnormal cell growth, such as cancer, in mammals by administering the compounds of formula 1 and to pharmaceutical compositions for treating such disorders which contain the compounds of formula 1. The invention also relates to methods of preparing the compounds of formula 1.

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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. Formula (I), wherein A is selected from among a single bond, =CH-, -CH2-, -O-, -S-, and -NH-; wherein n is 1, 2 or 3; wherein Z is C or N, the other variables are as defined in the claims, as well as in form of their acid addition salts with pharmacologically acceptable acids

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