- FUNGICIDAL OXADIAZOLES
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Disclosed are compounds of Formula 1, including all geometric and stereoisomers, tautomers, N-oxides, and salts thereof, wherein R1, L and J are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.
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Paragraph 0648-0649
(2020/06/07)
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- BENZIMIDAZOLE COMPOUNDS AND USE THEREOF FOR TREATING ALZHEIMER'S DISEASE OR HUNTINGTON'S DISEASE
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Benzimidazole compounds of formula (I), shown below, are disclosed. The compounds are potent human glutaminyl cyclase inhibitors. Also disclosed is a pharmaceutical composition containing one of these compounds and a pharmaceutical acceptable carrier, as well as a method of treating Alzheimer's disease or Huntington's disease by administering to a subject in need thereof an effective amount of such a compound.
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- BENZIMIDAZOLE COMPOUNDS AND USE THEREOF FOR TREATING ALZHEIMER'S DISEASE OR HUNTINGTON'S DISEASE
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Benzimidazole compounds of formula (I), shown below, are disclosed. The compounds are potent human glutaminyl cyclase inhibitors. Also disclosed is a pharmaceutical composition containing one of these compounds and a pharmaceutical acceptable carrier, as well as a method of treating Alzheimer's disease or Huntington's disease by administering to a subject in need thereof an effective amount of such a compound.
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- Identification and Structure–Activity Relationship (SAR) of potent and selective oxadiazole-based agonists of sphingosine-1-phosphate receptor (S1P1)
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Agonism of S1P1 receptor has been proven to be responsible for peripheral blood lymphopenia and elicts the identification of various S1P1 modulators. In this paper we described a series of oxadiazole-based S1P1 direct-acting agonists disubstituted on terminal benzene ring, with high potency for S1P1 receptor and favorable selectivity against S1P3 receptor. In addition, two representative agents named 16-3b and 16-3g demonstrated impressive efficacy in lymphocyte reduction along with reduced effect on heart rate when orally administered. Furthermore, these compounds have been shown to possess desired pharmacokinetic (PK) and physicochemical profiles. The binding mode between 16-3b and the activated S1P1 model was also studied.
- Liu, Tianqi,Jin, Jing,Chen, Yonghui,Xi, Qiumu,Hu, Jinping,Jia, Wenqiang,Chen, Xiaoguang,Li, Yan,Wang, Xiaojian,Yin, Dali
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- Carboxylic acid compound containing diphenyl oxadiazole, and preparation method and medical application of compound
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The invention relates to the field of medicinal chemistry, and particularly relates to a carboxylic acid compound (I) containing a diphenyl oxadiazole skeleton, a preparation method and pharmaceuticalpreparation of the compound, and a use of the compound
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- FUNGICIDAL OXADIAZOLES
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Disclosed are compounds of Formula 1, including all geometric and stereoisomers, tautomers, N-oxides, and salts thereof, wherein R1, A, and J are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.
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- Sphingol-1-phosphoric acid receptor modulator compound as well as preparation method and application thereof
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The invention relates to a sphingol-1-phosphoric acid receptor modulator compound as well as a preparation method and application thereof, and specifically provides the compound shown in the formula (I), a racemate thereof, a stereisomer, a tautomer, a solvate, an aquo-complex or pharmacologically acceptable salt thereof. The formula is shown in the description.
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- Low molecular weight dual inhibitors of factor Xa and fibrinogen binding to GPIIb/IIIa with highly overlapped pharmacophores
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Dual antithrombotic agents acting as anticoagulants and aggregation inhibitors could have substantial advantages over currently prescribed combinations of antithrombotic drugs. Herein, we report compounds with moderate inhibitory activity for factor Xa an
- Trstenjak, Uro?,Ila?, Janez,Kikelj, Danijel
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supporting information
p. 302 - 313
(2013/07/27)
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- PYRAZOLE-I, 2, 4 -OXAD IAZOLE DERIVATIVES AS S.PHING0SINE-1-PH0SPHATE AGONISTS
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Disclosed are compounds of Formula (I) or a pharmaceutically acceptable salt thereof, wherein: n is zero or an integer selected from 1 through 4; R1 is cycloalkyl, aryl, heteroaryl, or heterocyclyl, each optionally substituted with one to five substituents independently selected from C1 to C6 alkyl, C1 to C4 haloalkyl, benzyl, OR4, and/or halogen; and R2, R3, R4, and n are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
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Page/Page column 48
(2010/08/08)
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- Amine Compounds
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There is provided a compound exhibiting an activity of suppressing immune response with reduced adverse drug reactions, which compound is useful in the chemotherapy for preventing or treating, for example, a wide range of various autoimmune diseases including systemic erythematodes, chronic rheumatoid arthritis, Type I diabetes, inflammatory bowel disease, biliary cirrhosis, uveitis, multiple sclerosis or other disorders, or chronic inflammatory diseases, or cancers, lymphoma or leukemia, or resistance to organ or tissue transplantation or rejection against transplantation. Novel amine compounds having an S1P1/Edg1 receptor agonist effect, possible stereoisomers or racemic bodies of the compounds, or pharmacologically acceptable salts, hydrates or solvates of the compound, the stereoisomers or the racemic bodies, or prodrugs of the compounds, the stereoisomers, the racemic bodies, the salts, the hydrates or the solvates, are provided.
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Page/Page column 171
(2008/12/08)
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- A simple and efficient synthesis of new mono- and bis([1,2,4]-oxadiazol)- benzaldehyde building blocks
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An efficient approach to bis([1,2,4]-oxadiazol)benzaldehydes as well as the corresponding mono-benzaldehyde derivatives has been developed starting from benzamidoxime, which is readily obtained from 4-cyanobenzaldehyde. All these new compounds were synthe
- Crestey, Francois,Lebargy, Cyril,Lasne, Marie-Claire,Perrio, Cecile
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p. 3406 - 3410
(2008/09/20)
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