84089-73-6Relevant academic research and scientific papers
Anti-influenza virus compound as well as preparation method and application thereof
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Paragraph 0131; 0134; 0136, (2021/05/01)
The invention provides an anti-influenza virus pharmaceutical compound, and a preparation method and application thereof. The compound provided by the invention is a prodrug, has remarkably improved bioavailability and antiviral activity compared with a parent drug, is suitable for treating/prepaid influenza virus infection related diseases, has improved pharmacokinetic characteristics, and is particularly suitable for being developed into an oral preparation.
SUBSTITUTED QUINOLIZINE DERIVATIVES USEFUL AS HIV INTEGRASE INHIBITORS
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Page/Page column 30; 31, (2018/08/20)
The present invention relates to Substituted Quinolizine Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein R1 is as defined herein. The present invention also relates to compositions comprising at least one Substituted Quinolizine Derivative, and methods of using the Substituted Quinolizine Derivatives for treating or preventing HIV infection in a subject.
A 1 - iodo ethyl isopropyl carbon ester preparation method (by machine translation)
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Paragraph 0011; 0012, (2017/06/08)
The invention discloses cephalosporins antibiotics of cefpodoxime proxetil intermediate 1 - iodo ethyl isopropyl carbon ester preparation method, will 1 - chloro ethyl isopropyl carbonate is dissolved in ethyl acetate, adds the sodium iodide, TBAB, calcium chloride heating reflux reaction 3h to obtain the target product 1 - iodo ethyl isopropyl carbonate, sample gas-phase detection purity _aogtao_ 95%, the yield of the crude mole _aogtao_ 90%, without passing through the distillation can be directly used for the next step synthesis. The invention synthetic product high purity, high yield and does not require the high vacuum distillation can be directly synthesizing the next step, for large-scale production and cost of cefpodoxime proxetil control provides a guarantee. (by machine translation)
NEP inhibitor and medicine composition thereof
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Paragraph 0073; 0074; 0075; 0076, (2017/07/26)
The invention relates to an NEP inhibitor and a medicine composition thereof, and in particular, relates to a (2R,4S)-5-([1,1'-biphenyl]-4-yl)-4-(3-carboxylpropionylamino)-2-methylpentanoate derivative represented as the formula (I), and a stereoisomer, a hydrate or a solvate thereof, and a medicine composition thereof, wherein the substituent groups in the formula (I) are defined as same as the specification. The series of the compounds in the invention have significant NEP inhibition activity, good solubility and high bioavailability, and can be used for developing medicines used in therapy or prevention of hypertension, pulmonary arterial hypertension, heart failure, kidney diseases and the like, which are related to NEP abnormality, so that it is hopeful to develop a new-generation NEP inhibitor.
3,3-DISUBSTITUTED-1-HYDROXYTRIAZ-1-ENE 2-OXIDES AND WOUND-HEALING COMPOSITIONS USING THEM
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Paragraph 00129, (2015/08/03)
Esters, carbonates and imides of 3,3-disubstituted-1-hydroxytriaz-1-ene 2-oxides of the formula I are disclosed. The compounds release nitric oxide (NO) under physiologic conditions, and pharmaceutical compositions containing them are useful to aid in wound healing.
NO-RELEASING NONOATE (NITROGEN-BOUND) SULFONAMIDE-LINKED-COXIB ANTI-CANCER AGENTS
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Paragraph 00161; 00162, (2014/02/15)
The present invention provides NO-releasing NONOate(nitrogen bound)sulfonamide- linked-coxib anti-cancer agents, having the structure of Formula (I): wherein R1, X, L, R2, R3, R4, and Z are as defined in the detailed description; pharmaceutical compositions comprising at least one compound of Formula (I); and methods useful for healing wounds, preventing and treating cancer, or treating actinic keratosis, cystic fibrosis or acne, using a compound of Formula (I).
CYCLOALKYL-SUBSTITUTED IMIDAZOLE DERIVATIVE
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Paragraph 0375-0377, (2013/03/26)
A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof, wherein A represents a C3 to C12 cycloalkyl group which may be substituted by one to three selected from a fluoro group, a hydroxy group, a C1 to C6 alkyl group, etc; R1, R2, and R3 each independently represent a hydrogen atom, a fluoro group, or a C1 to C6 alkyl group; R4 represents a hydrogen atom or a prodrug group; and Y represents -CH2-CHR5-CH2-NHR6 (wherein R5 represents a hydrogen atom, a C1 to C6 alkyl group, or a C1 to C6 alkoxy group, and R6 represents a hydrogen atom or a prodrug group), or the like exhibits excellent TAFIa inhibitory activity and is useful as a therapeutic drug for myocardial infarction, angina pectoris, acute coronary syndrome, cerebral infarction, deep vein thrombosis, pulmonary embolism, and the like.
NOVEL BETULINIC ACID DERIVATIVES AS HIV INHIBITORS
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Paragraph 0169, (2013/11/18)
(I)The invention relates to novel novel betulinic acid derivatives and related compounds, and pharmaceutical compositions useful for therapeutic treatment of viral diseases and particularly HIV mediated diseases.
N-SUBSTITUTED-CYCLIC AMINO DERIVATIVE
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Page/Page column 161, (2012/05/20)
The present invention provides a compound of formula (I): wherein R1a is optionally substituted C1-6 alkyl, etc.; R1m is hydrogen atom, etc.; G1, G2, G3 and G4 are (i), etc. ((i) G1 is -N(R1b)-, G2 is -CO-, G3 is -C(R1c)(R1d)-, and G4 is oxygen, etc.); R1b is optionally substituted C1-6 alkyl, etc.; R1c and R1d are each independently optionally substituted C1-6 alkyl, etc.; R2 is optionally substituted C1-6 alkyl, etc.; R3a, R3b, R3c, and R3d are each independently a group: -A-B (A is a single bond, etc., B is hydrogen atom, etc.), etc.; n is 1, etc.; R5 is C1-4 alkoxycarbonyl, etc., or a pharmaceutically acceptable salt thereof, which is useful as a renin inhibitor.
Synthesis and biological evaluation of orally active hypolipidemic agents
Bandgar, Babasaheb P.,Sarangdhar, Rajendra J.,Khan, Fruthous,Mookkan, Jeyamurugan,Shetty, Pranesha,Singh, Gajendra
experimental part, p. 5915 - 5926 (2011/10/08)
A series of novel fenofibric acid ester prodrugs 1c-1h were synthesized and evaluated with the aim of obtaining potent hypolipidemic agents. Prodrugs 1c and 1d exhibited potent hypochlolesterolemic activity, lowering the mice plasma triglyceride level up to 47% in Swiss albino mice after oral administration of 50 mg/kg/day for 8 days. Fenofibric acid ester prodrugs 1c-1h were found lipophilic like fenofibrate (1b), indicated by partition coefficients measured in octanol-buffer system at pH 7.4. On the basis of in vivo studies, prodrugs 1c and 1d emerged as potent hypolipidemic agents.
