- Fused tetracyclic compounds and application thereof in medicines
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The invention relates to fused tetracyclic compounds and an application thereof in medicines, and in particular, relates to the application of the fused tetracyclic compounds as medicines for treatingand/or preventing hepatitis B. Specifically, the invention relates to the compounds represented by a general formula (I) or stereoisomers, tautomers, nitrogen oxides, solvates, metabolites, pharmaceutically acceptable salts or prodrugs thereof, wherein the variables are defined in the specification. The invention further relates to the application of the compounds represented by the general formula (I) or the stereoisomers, the tautomers, the nitric oxides, the solvates, the metabolites, the pharmaceutically acceptable salts or the prodrugs thereof as medicines, and in particular, relates tothe application of the compounds as the medicines for treating and/or preventing hepatitis B.
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Paragraph 0677; 0679-0682
(2020/04/17)
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- PqsR INVERSE AGONISTS
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The present invention relates to a compound according to general formula (I), which acts as an inhibitor of PqsR (the currently only known receptor for the Pseudomonas Quinolone Signal (PQS)); to a pharmaceutical composition containing one or more of the compound(s) of the invention; to a combination preparation containing at least one compound of the invention and at least one further active pharmaceutical ingredient; and to uses of said compound(s), including the use as a medicament, e.g. the use in the treatment or prophylaxis of a bacterial infection, especially a Pseudomonas aeruginosa or Burkholderia infection.
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Page/Page column 52; 55; 57; 58; 59
(2020/01/31)
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- COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH NLRP ACTIVITY
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In one aspect, compounds of Formula A, or a pharmaceutically acceptable salt thereof, are featured (Formula A) or a pharmaceutically acceptable salt thereof, wherein the variables shown in Formula A can be as defined anywhere herein.
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Page/Page column 278-279
(2020/06/10)
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- Preparation method of 2-(2-bromo-1,3-thiazol-5-yl) acetonitrile
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The invention discloses a preparation method of 2-(2-bromo-1,3-thiazol-5-yl) acetonitrile, which comprises the following steps: S1) adding a first organic solvent and methyl 2-bromothiazole-4-carboxylate into a reaction flask, cooling the mixture to 0 DEG C, adding sodium borohydride, reacting the mixture at room temperature, performing concentration and extraction, combining organic phases, and performing concentration and column chromatography separation to obtain 2-bromothiazole-5-methanol; S2) adding a second organic solvent and the 2-bromothiazole-5-methanol into a reaction bottle, cooling the mixture to 0 DEG C, adding phosphorus tribromide, washing a product with mother liquor, and performing concentration to obtain 2-bromo-5-bromomethyl-thiazole; S3) adding acetonitrile, the 2-bromo-5-bromomethyl-thiazole, potassium carbonate, tetrabutylammonium fluoride and TMSCN sequentially into a reaction flask, performing extraction, combining organic phases, and performing concentration and recrystallization to obtain the 2-(2-bromo-1,3-thiazol-5-yl) acetonitrile. The preparation method breaks through the blank at home and abroad, the preparation process and purification steps are safe and simple, and the preparation method is suitable for industrial production.
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Paragraph 0021-0024; 0030-0032; 0038-0040
(2019/12/02)
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- SULPHONAMIDES AND COMPOSITIONS THEREOF FOR TREATING CONDITIONS ASSOCIATED WITH NLRP ACTIVITY
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In one aspect, compounds of Formula AA, or a pharmaceutically acceptable salt thereof, are featured: wherein the variables shown in Formula AA can be as defined anywhere herein. Compounds AA are modulators of NLRP1 and/or NLRP3
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Page/Page column 460
(2019/05/10)
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- Hetero-aromatic compound and its use in medicine
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The invention provides a hetero-aromatic compound or a stereisomer, geometric isomer, tautomer, despinner, nitrogen oxide, hydrate, solvate, metabolite, metabolism precursor and pharmaceutically acceptable salt or prodrug thereof, which is used for treating proliferative diseases. The invention also discloses a pharmaceutical composition containing the compound and an application of the compound or pharmaceutical composition thereof in preparation of a medicine for treating proliferative diseases.
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Paragraph 1729; 1743-1745
(2019/07/04)
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- SUBSTITUTED NITROGEN CONTAINING COMPOUNDS
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Disclosed are compounds of Formula (I): or a salt thereof, Formula (II) wherein R1 is: or; each W is independently NR1b or O; Z is a bond or CHR1d; and R1, R2, Rd, R3a, R3b, L1, B, V, Y, and n are defined herein. Also disclosed are methods of using such compounds as inhibitors of ROMK, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating cardiovascular diseases.
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Page/Page column 83
(2019/01/05)
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- HEPATITIS C INHIBITORS AND USES THEREOF
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This disclosure relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.
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Page/Page column 125-126
(2012/07/13)
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- The discovery of high affinity agonists of GPR109a with reduced serum shift and improved ADME properties
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Amino-anthranilic acid derivatives have been identified as a new class of low serum shifted, high affinity full agonists of the human orphan G-protein-coupled receptor GPR109a with improved ADME properties.
- Imbriglio, Jason E.,Dirocco, Daniel,Bodner, Rena,Raghavan, Subharekha,Chen, Weichun,Marley, Daria,Esser, Craig,Holt, Tom G.,Wolff, Michael S.,Taggart, Andrew K.P.,Waters, M. Gerard,Tata, James R.,Colletti, Steven L.
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supporting information; scheme or table
p. 2721 - 2724
(2011/06/20)
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- AMINOTRIAZOLE DERIVATIVES AS ALX AGONISTS
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The invention relates to aminotriazole derivatives of formula (I), wherein A, E, R1 and R2 are as defined in the description, their preparation and their use as pharmaceutically active compounds. The compounds are useful for the prevention or treatment of diseases, which respond to the modulation of the ALX receptor such as inflammatory diseases.
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Page/Page column 92
(2009/07/18)
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- NOVEL COMPOUNDS FOR THE TREATMENT OF DISEASES ASSOCIATED WITH AMYLOID OR AMYLOID-LIKE PROTEINS
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The present invention relates to novel compounds that can be employed in the treatment of a group of disorders and abnormalities associated with amyloid protein, such as Alzheimer's disease, and of diseases or conditions associated with amyloid-like proteins. The compounds of the present invention can also be used in the treatment of ocular diseases associated with pathological abnormalities/changes in the tissues of the visual system. The present invention further relates to pharmaceutical compositions comprising these compounds and to the use of these compounds for the preparation of medicaments for treating or preventing diseases or conditions associated with amyloid and/or amyloid-like proteins. A method of treating or preventing diseases or conditions associated with amyloid and/or amyloid-like proteins is also disclosed.
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Page/Page column 61
(2008/12/05)
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- Ranging correlated motion (1.5 nm) of two coaxially arranged rotors mediated by helix inversion of a supramolecular transmitter
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For a long-range transmission of motion between two movable parts apart from each other, transmitters that can precisely correlate these two motions should be properly incorporated into the system. However, such a motional relay is yet to be realized in a
- Hiraoka, Shuichi,Okuno, Erika,Tanaka, Takaaki,Shiro, Motoo,Shionoya, Mitsuhiko
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supporting information; experimental part
p. 9089 - 9098
(2009/02/03)
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- HETEROCYCLYL-SUBSTITUTED ANTI-HYPERCHOLESTEROLEMIC COMPOUNDS
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This invention provides cholesterol absorption inhibitors of Formula I: and the pharmaceutically acceptable salts thereof, wherein R12 is a hydroxylated alkyl group and R9 contains a heterocyclic ring. The compounds are useful for lowering plasma cholesterol levels, particularly LDL cholesterol, and for treating atherosclerosis and preventing atherosclerotic disease events.
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Page/Page column 40
(2008/12/05)
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- PYRIDINONYL PDK1 INHIBITORS
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The present invention provides pyridinonyl PDKl inhibitors and methods of treating cancer using the same.
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Page/Page column 86
(2008/06/13)
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- Discovery of biaryl anthranilides as full agonists for the high affinity niacin receptor
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Biaryl anthranilides are reported as potent and selective full agonists for the high affinity niacin receptor GPR109A. The SAR presented outlines approaches to reduce serum shift and both CYPCYP2C8 and CYP2C9 liabilities, while improving PK and maintainin
- Shen, Hong C.,Ding, Fa-Xiang,Luell, Silvi,Forrest, Michael J.,Carballo-Jane, Ester,Wu, Kenneth K.,Wu, Tsuei-Ju,Cheng, Kang,Wilsie, Larissa C.,Krsmanovic, Mihajlo L.,Taggart, Andrew K.,Ren, Ning,Cai, Tian-Quan,Deng, Qiaolin,Chen, Qing,Wang, Junying,Wolff, Michael S.,Tong, Xinchun,Holt, Tom G.,Waters, M. Gerard,Hammond, Milton L.,Tata, James R.,Colletti, Steven L.
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p. 6303 - 6306
(2008/04/12)
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- NIACIN RECEPTOR AGONISTS, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF TREATMENT
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The present invention encompasses compounds of Formula (I): as well as pharmaceutically acceptable salts and hydrates thereof, that are useful for treating atherosclerosis, dyslipidemias and the like. Pharmaceutical compositions and methods of use are also included.
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Page/Page column 25; 37-39
(2008/06/13)
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- Niacin receptor agonists, compositions containing such compounds and methods of treatment
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The present invention encompasses compounds of Formula I: as well as pharmaceutically acceptable salts and hydrates thereof, that are useful for treating atherosclerosis, dyslipidemias and the like. Pharmaceutical compositions and methods of use are also included.
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Page/Page column 23; 42
(2010/11/25)
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- 1-ACYL-PYRROLIDINE DERIVATIVES FOR THE TREATMENT OF VIRAL INFECTIONS
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Anti-viral agents of Formula (I) wherein: A represents hydroxy; D represents aryl or heteroaryl; E represents hydrogen, C1-6alkyl, aryl, heteroaryl or heterocyclyl; G represents hydrogen or optionally substituted C1-6alkyl; J represents C1-6alkyl, heteroc
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Page 69 - 70
(2008/06/13)
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