173604-87-0Relevant articles and documents
PRODRUGS OF THE TYROSINE KINASE INHIBITOR FOR TREATING CANCER
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Paragraph 00189-00190, (2021/03/05)
There are provided compounds of Formula (I), and pharmaceutically acceptable salts and esters thereof, and pharmaceutical compositions thereof, useful for inhibition or modulation of the activity of tyrosine kinases and treatment of disease states or conditions mediated by tyrosine kinases, including cancers. (I)
GLYCYRRHETINIC ACID DERIVATIVES FOR USE IN TREATING HYPERKALEMIA
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Page/Page column 179, (2020/08/22)
The present invention provides a compound of formula (I) or a salt thereof: (F ormula (I)) wherein X, L, V, R1, R2, R3 and R4, are as defined herein. The claimed compounds inhibit the enzyme 11-hydroxysteroid de
DERIVATIVES OF RELEBACTAM AND USES THEREOF
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Paragraph 1364-1366; 1766-1767, (2020/04/24)
Derivatives of relebactam, therapeutic methods of using the derivatives of relebactam, particularly in combination with β-lactam antibiotics and pharmaceutical compositions thereof are disclosed. The derivatives of relebactam are suitable for oral administration.
Influenza virus replication inhibitors and uses thereof (by machine translation)
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Paragraph 0742; 0744-0746, (2019/10/01)
The invention provides a compound as an influenza virus replication inhibitor, a method for preparing the same, a pharmaceutical composition containing the compound and application. (by machine translation)
Coupling of an Acyl Migration Prodrug Strategy with Bio-activation to Improve Oral Delivery of the HIV-1 Protease Inhibitor Atazanavir
Subbaiah, Murugaiah A. M.,Meanwell, Nicholas A.,Kadow, John F.,Subramani, Lakshumanan,Annadurai, Mathiazhagan,Ramar, Thangeswaran,Desai, Salil D.,Sinha, Sarmistha,Subramanian, Murali,Mandlekar, Sandhya,Sridhar, Srikanth,Padmanabhan, Shweta,Bhutani, Priyadeep,Arla, Rambabu,Jenkins, Susan M.,Krystal, Mark R.,Wang, Chunfu,Sarabu, Ramakanth
, p. 4176 - 4188 (2018/05/23)
HIV-1 protease inhibitors (PIs), which include atazanavir (ATV, 1), remain important medicines to treat HIV-1 infection. However, they are characterized by poor oral bioavailability and a need for boosting with a pharmacokinetic enhancer, which results in additional drug-drug interactions that are sometimes difficult to manage. We investigated a chemo-activated, acyl migration-based prodrug design approach to improve the pharmacokinetic profile of 1 but failed to obtain improved oral bioavailability over dosing the parent drug in rats. This strategy was refined by conjugating the amine with a promoiety designed to undergo bio-activation, as a means of modulating the subsequent chemo-activation. This culminated in a lead prodrug that (1) yielded substantially better oral drug delivery of 1 when compared to the parent itself, the simple acyl migration-based prodrug, and the corresponding simple l-Val prodrug, (2) acted as a depot which resulted in a sustained release of the parent drug in vivo, and (3) offered the benefit of mitigating the pH-dependent absorption associated with 1, thereby potentially reducing the risk of decreased bioavailability with concurrent use of stomach-acid-reducing drugs.
Tetrahydrocyclopentapyrrole derivative and preparation method therefor
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, (2016/10/08)
The purpose of the present invention is to provide: a tetrahydrocyclopentapyrrole derivative capable of being used for preventing or treating a peptic ulcer gastritis or reflux esophagitis; a preparation method therefor; and a pharmaceutical composition containing the same.
Pharmaceutical composition for the treatment or prevention of stroke and systemic embolism
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Paragraph 0532-0536, (2016/11/17)
The present invention relates to a prodrug useful for treating or preventing a stroke and systemic embolism and suitable for being effectively used in the oral delivery of dabigatran, and to a compound represented by chemical formula 1, a pharmaceutically acceptable salt thereof, and a hydrate thereof or a solvate thereof. The compound represented by the chemical formula 1, the pharmaceutically acceptable salt thereof, and the hydrate thereof or the solvate thereof are useful for treating or preventing a stroke and systemic embolism, and is suitable for being effectively used in oral delivery since the absorption rate, that is, bioavailability of dabigatran is improved.(AA) DSC curve of dabigatran pivoxyl (+)-(1S)- campo-10-sulfonateCOPYRIGHT KIPO 2015
N-SUBSTITUTED-CYCLIC AMINO DERIVATIVE
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Page/Page column 159, (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.
NITROGEN CONTAINING HETEROAROMATICS AS FACTOR Xa INHIBITORS
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Page/Page column 78, (2009/10/01)
The present application describes nitrogen containing heteroaromatics and derivatives thereof of formula (I) or pharmaceutically acceptable salt or prodrug forms thereof, wherein J is N or NH and D may be C(=NH)NH2, which are useful as inhibitors of factor Xa.
9-Aminocarbonylsubstituted derivatives of glycylcyclines
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Page/Page column 47, (2010/11/26)
This invention provides compounds of Formula I having the structure where R1, R2, R3 and A are defined in the specification or a pharmaceutically acceptable salt thereof useful as antibacterial agents. Compounds according