- PYRIDINE COMPOUND SUBSTITUTED WITH AZOLE
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The present invention provides a compound represented by formula [I] shown below or a pharmaceutically acceptable salt thereof that has an inhibitory effect on 20-HETE producing enzyme. (in formula [I] above, the structure represented by formula [II] below: represents any of the structures represented by formula group [III] below: R1, R2, R3, and R4 independently represent a hydrogen atom, a fluorine atom, methyl, or the like, R5 represents any of the structures represented by formula group [IV]:
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Paragraph 0917; 1089
(2020/07/07)
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- Biphenyl compound as well as preparation method and medical application thereof
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The invention discloses a biphenyl compound as well as a preparation method and medical application thereof, the structure of the biphenyl compound is shown as a formula (I) or a formula (II), and thebiphenyl compound or pharmaceutically acceptable salt, tautomer, meso-isomer, raceme, stereoisomer, metabolite, metabolite precursor, prodrug or solvate thereof is a PD-L1 inhibitor. The compound hasa remarkable inhibiting effect on the interaction of PD-1 and PD-L1 protein, so that the compound can be applied to the preparation of PD-L1 inhibitors and immunomodulator drugs for preventing or treating tumors, autoimmune diseases, organ transplant rejection, infectious diseases and inflammatory diseases.
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Paragraph 1202-1208
(2020/11/22)
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- PD-1/PD-L1 INHIBITORS
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Compounds according to formula (I), methods of using said compounds singly or in combination with additional agents and compositions of said compounds for the treatment of cancer are disclosed.
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Page/Page column 454
(2018/11/22)
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- Enantioselective Total Synthesis of Beraprost Using Organocatalyst
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A convergent and enantioselective total synthesis of the most active isomer of beraprost was achieved in 17 pots. A unique tricyclic core in beraprost was synthesized efficiently by utilizing the asymmetric organocatalyst-mediated formal [3 + 2] cycloaddi
- Umemiya, Shigenobu,Sakamoto, Daisuke,Kawauchi, Genki,Hayashi, Yujiro
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supporting information
p. 1112 - 1115
(2017/03/14)
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- Substituted 1-benzylcycloalkylcarboxylic acids and the use thereof
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The present application relates to novel substituted 1-benzylcycloalkylcarboxylic acid derivatives, to processes for their preparation, to their use for the treatment and/or prevention of diseases, and to their use for producing medicaments for the treatment and/or prevention of diseases, especially for the treatment and/or prevention of cardiovascular disorders.
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Page/Page column 19
(2012/07/14)
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- 8-AZABICYCLO[3.2.1]OCTANE-8-CARBOXAMIDE DERIVATIVE
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Disclosed is a compound represented by formula (1) or a pharmacologically acceptable salt thereof (In the formula, A represents a group that is represented by formula (A-1); R1a and R1b may be the same or different and each independently represents a C1-6 alkyl group which may be substituted by one to three halogen atoms; m and n each independently represents an integer of 0-5; X1 represents a hydroxyl group or an aminocarbonyl group; Z1 represents a single bond or the like; and R2 represents an optionally substituted C1-6 alkyl group, an optionally substituted C6-10 aryl group or the like.)
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Page/Page column 46
(2012/09/11)
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- POLYSUBSTITUTED DERIVATIVES OF 2-ARYL-6-PHENYL-IMIDAZO[1,2-a]PYRIDINES, AND PREPARATION AND THERAPEUTIC USE THEREOF
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Compounds of formula (I): wherein R1, R2, R3, R4 and X are as defined in the disclosure, or an acid addition salt thereof, and the therapeutic use and process of synthesis thereof.
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Page/Page column 11
(2011/04/18)
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- OXO-HETEROCYCLIC SUBSTITUTED CARBOXYLIC ACID DERIVATIVES AND THE USE THEREOF
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The present application relates to novel carboxylic acid derivatives having an oxo-substituted azaheterocyclic partial structure, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for producing medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prevention of cardiovascular disorders.
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Page/Page column 96
(2011/02/26)
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- Discovery of potent, selective, and orally bioavailable alkynylphenoxyacetic acid CRTH2 (DP2) receptor antagonists for the treatment of allergic inflammatory diseases
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New phenoxyacetic acid antagonists of CRTH2 are described. Following the discovery of a hit compound by a focused screening, high protein binding was identified as its main weakness. Optimization aimed at reducing serum protein binding led to the identification of several compounds that showed not only excellent affinities for the receptor (41 compounds with Ki 50 100 nM; PGD2-induced eosinophil shape change). Additional optimization of the PK characteristics led to the identification of several compounds suitable for in vivo testing. Of these, 19k and 19s were tested in two different pharmacological models (acute FITC-mediated contact hypersensitivity and ovalbumin-induced eosinophilia models) and found to be active after oral dosing (10 and 30 mg/kg).
- Crosignani, Stefano,Prêtre, Adeline,Jorand-Lebrun, Catherine,Fraboulet, Ga?le,Seenisamy, Jeyaprakashnarayanan,Augustine, John Kallikat,Missotten, Marc,Humbert, Yves,Cleva, Christophe,Abla, Nada,Daff, Hamina,Schott, Olivier,Schneider, Manfred,Burgat-Charvillon, Fabienne,Rivron, Delphine,Hamernig, Ingrid,Arrighi, Jean-Fran?ois,Gaudet, Marilène,Zimmerli, Simone C.,Juillard, Pierre,Johnson, Zoe
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supporting information; experimental part
p. 7299 - 7317
(2011/12/15)
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- PHENOXY ACETIC ACID DERIVATIVES
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The present invention provides phenoxyacetic acid derivatives of Formula (I) for the treatment of CRTH2 related disorders and disease selected from asthma, atopic dermatitis and inflammatory dermatoses.
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Page/Page column 63
(2010/09/03)
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- PYRAZOLE DERIVATIVES AS 5-LO INHIBITORS
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The invention relates to compounds of formula (I) processes for their preparation, their use as 5-lipoxygenase inhibitors and pharmaceutical compositions containing the same.
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Page/Page column 85-86
(2009/07/03)
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- Compounds and Methods for Inhibiting the Interaction of BCL Proteins with Binding Partners
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The invention relates to isoxazolidine containing compounds that bind to bcl proteins and inhibit Bcl function. The compounds may be used for treating and modulating disorders associated with hyperproliferation, such as cancer.
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Page/Page column 119
(2008/12/05)
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- Discovery of selective metal-binding peptoids using 19F encoded combinatorial libraries
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A method for encoding solid-phase split/mix combinatorial libraries using the chemical shift of synthetic fluoroarenes ('F-codes') has been developed. They have wide chemical shift dispersion and are detectable at the sub-μmol level. 19F NMR is
- Pirrung, Michael C.,Park, Kaapjoo
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p. 2115 - 2118
(2007/10/03)
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