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The present invention concerns the compounds having the formula N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs esters and metabolites thereof. It further relates to their use as broadspectrum HIV protease inhibitors, processes for their preparation as well as pharmaceutical compositions and diagnostic kits comprising them. It also concerns combinations thereof with another anti-retroviral agent, and to their use in assays as reference compounds or as reagents.

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This invention relates to compounds, in particular benzimidazoles, that are useful as estrogen agonists and/or antagonists and pharmaceutical uses thereof. The present invention also relates to benzimidazoles that are selective for the ERbeta receptor and pharmaceutical uses thereof.

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The present invention refers to a fullerene derivative is denoted by chemical formula 1 a, or a pharmaceutically acceptable salt including and is directed to pharmaceutical composition. The present invention according to that it represents a kinase inhibitory activity FMS compounds, as well as the associated for preventing or treating disease pharmaceutical compositions can be used. [Formula 1] In formula said, R 1 and R 2 definition of is defined specification. (by machine translation)

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Cycloalkylcarbonylamino acid derivatives, which are raw material intermediates of a novel cycloalkane carboxamide derivative that selectively inhibits cathepsin K, and a production process thereof, are provided. A cycloalkylcarbonylamino acid derivative represented by the following general formula (I), or a pharmaceutically acceptable salt thereof: (wherein, R1 and R2 represent alkyl groups, alkenyl groups, alkynyl groups, aromatic hydrocarbon groups, heterocyclic groups or the like, and ring A represents a cyclic alkylidene group having 5, 6 or 7 carbon atoms).

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The invention relates to new azetidine derivatives of the formula 1 to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them

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The present invention discloses novel compounds inhibiting LRRK2 kinase activity, the preparation processes thereof, the compositions containing them, as well as the use in treating diseases characterized by LRRK2 kinase activity, particularly Parkinson¿s disease and Alzheimer¿s disease

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Described herein is a novel series of multi-fluoro-substituted pyrazolopyrimidine compounds or salts thereof. These compounds are Bruton’s tyrosine kinase (BTK) inhibitors. These compounds may possess better BTK inhibition selectivity and pharmacokinetic properties. Disclosed herein are the synthesis methods of these compounds. Disclosed herein are novel synthesis methods of the multi-fluoro-substituted benzophenone and substituted phenoxy benzene. Also disclosed are pharmaceutical compositions comprising the BTK inhibitors described herein. The present invention also relates to pharmaceutical formulations comprising the compounds described herein as active ingredients. The present invention also includes the therapeutic methods by administering the BTK inhibitors and their formulations to treat and inhibit autoimmune disease, hypersensitivity disease, inflammatory diseases and cancer.

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Disclosed is an isoxazole derivative that inhibits the activity of the Janus kinases (JAKs), the structure thereof as presented in formula I, formula II, formula IX, and formula XI. The substituent groups in the formulas are described in the description. Also disclosed are the pharmaceutical composition of the compound and a related use in medicine preparation.

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A highly efficient and milder protocol for the syntheses of novel series of 2-aminothiazoles bearing 5-methylisoxazoline and pyridine-piperazine hybrid molecules has been developed. The target compounds 13a-e were screened for their in vitro cytotoxicity activity against various tumor cell lines including MCF-7 (human breast adenocarcinoma), HCT-116 (colorectal carcinoma), Jurkat (human T-cell leukemia) and THP-1 (human acute monocytic leukemia). The bioactive assay showed that the most of the new compounds exhibited promising results in comparison with the parental Sunitinib. The synthesized compounds could well be used in the future as lead anticancer drugs in drug development studies. The synthesized compounds were fully characterized by IR,1 H NMR,13 C NMR, elemental analysis and mass spectral data.

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Reference:
Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem

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Compounds of the following formula have pharmaceutical properties: STR1 in which X is R'(HO)C=C(CN)–, R1 (CO)–CH(CN)– or STR2 R1 and R2 are each hydrogen or C1-6 alkyl, R3, R4, R5 and R6 are each hydrogen, hydroxy, halogen, nitro, cyano, carboxy, C1-4 alkyl, C1-4 alkoxy, C1-4 alkylthio, halo-substituted C1-4 alkyl, halo-substituted C1-4 alkoxy, halo-substituted C1-4 alkylthio, C2-5 alkoxycarbonyl, optionally substituted phenyl, optionally substituted phenoxy, R’R”N– where R’ and R” are each hydrogen or C1-4 alkyl or R'”CONH– where R'” is C1-4 alkyl, or a group of the formula –CR7 R8 R9 in which R7, R8 and R9 are each C1-6 alkyl, halo-substituted C1-6 alkyl or optionally substituted phenyl, or R7 and R8, together with the carbon atom to which they are attached, form a cycloalkyl group containing 3 to 7 carbon atoms, or R7, R8 and R9 together with the carbon atom to which they are attached, form a bicycloalkyl group containing 4 to 9 carbon atoms, and Y is a 5- or 6-membered heterocyclic ring excluding pyrazole; and salts thereof.

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Reference:
Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem