- Isoindoline scaffold-based dual inhibitors of HDAC6 and HSP90 suppressing the growth of lung cancer in vitro and in vivo
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This study reports the synthesis of a series of 2-aroylisoindoline hydroxamic acids employing N-benzyl, long alkyl chain and acrylamide units as diverse linkers. In-vitro studies led to the identification of N-benzyl linker-bearing compound (10) and long
- Ojha, Ritu,Nepali, Kunal,Chen, Chun-Han,Chuang, Kuo-Hsiang,Wu, Tung-Yun,Lin, Tony Eight,Hsu, Kai-Cheng,Chao, Min-Wu,Lai, Mei-Jung,Lin, Mei-Hsiang,Huang, Han-Li,Chang, Chao-Di,Pan, Shiow-Lin,Chen, Mei-Chuan,Liou, Jing-Ping
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- THIENODIAZEPINE DERIVATIVES AND APPLICATION THEREOF
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The present invention relates to a class of thienodiazepine derivatives and an application thereof in the preparation of a drug for the treatment of diseases associated with bromodomain and extra-terminal (BET) Bromodomain inhibitors. Specifically, the present invention relates to compounds represented by formulas (I) and (II), as well as pharmaceutically acceptable salts thereof.
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Paragraph 0186-0188
(2020/08/09)
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- COMPOUNDS FOR TREATMENT OF CARDIAC ARRHYTHMIAS AND HEART FAILURE
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This disclosure concerns compounds and a method for modulating the activity of calcium ion channels, including Ca2+-induced (or Ca2+-activated) calcium release channels and conformationally coupled calcium release channels such as ryanodine receptors. Some of the compounds have a structure according to formula I, or a stereoisomer, tautomer, hydrate, solvate, prodrug, or pharmaceutically acceptable salt thereof.
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Page/Page column 7
(2019/10/19)
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- HETEROARYL COMPOUNDS AND USES THEREOF
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The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same. It has now been found that compounds of this invention, and pharmaceutically acceptable compositions thereof, are effective as inhibitors of one or more protein kinases. Such compounds have general formula I or a pharmaceutically acceptable salt thereof, wherein Ring A, Ring B, W, Ry, R3 and R4 are as defined herein.
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- PYRIDONE AND AZA-PYRIDONE COMPOUNDS AND METHODS OF USE
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Pyridone and aza-pyridone compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
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Page/Page column 330
(2011/11/30)
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- THERAPEUTIC ANTIVIRAL PEPTIDES
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Disclosed herein are compounds represented by a formula: Therapeutic methods, compositions, medicaments, and dosage forms related thereto are also disclosed.
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- PREPARATION AND USES OF 1,2,4-TRIAZOLO [1,5a] PYRIDINE DERIVATIVES
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This application relates to compounds of the general Formula I and salts thereof, wherein X, R1A, R1B, R2, R3, R4, and R5 are as defined herein. The application also relates to compositions and methods of treatment of hyperproliferative diseases or disorders.
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Page/Page column 247; 248
(2010/12/29)
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- Inhibitors of dipeptidyl peptidase 8 and dipeptidyl peptidase 9. Part 2: Isoindoline containing inhibitors
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To obtain selective and potent inhibitors of dipeptidyl peptidases 8 and 9, we synthesized a series of substituted isoindolines as modified analogs of allo-Ile-isoindoline, the reference DPP8/9 inhibitor. The influence of phenyl substituents and different P2 residues on the inhibitors' affinity toward other DPPs and more specifically, their potential to discriminate between DPP8 and DPP9 will be discussed. Within this series compound 8j was shown to be a potent and selective inhibitor of DPP8/9 with low activity toward DPP II.
- Van Goethem, Sebastiaan,Van der Veken, Pieter,Dubois, Veronique,Soroka, Anna,Lambeir, Anne-Marie,Chen, Xin,Haemers, Achiel,Scharpe, Simon,De Meester, Ingrid,Augustyns, Koen
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scheme or table
p. 4159 - 4162
(2009/05/07)
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- COMPOSITIONS AND METHODS FOR INHIBITION OF THE JAK PATHWAY
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The invention encompasses compounds having formula I and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases are therapeutically useful.
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Page/Page column 118
(2008/12/05)
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- CETP INHIBITORS
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Compounds having the structure of Formula (I), including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In the compounds of Formula (I), B is a cyclic group other than phenyl, and B has a cyclic substituent at a position that is ortho to the position at which B is connected to the remainder of the structure of Formula (I). The 5-membered ring of Formula (I) has a second cyclic substituent in addition to B.
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Page/Page column 51-52
(2008/06/13)
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- CARBOXYAMINE COMPOUNDS AND METHODS OF USE THEREOF
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The invention relates to the use of carboxyamine compounds and salts thereof in the treatment of HDAC dependent diseases and for the manufacture of pharmaceutical preparations for the treatment of said diseases.
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Page/Page column 78
(2010/11/26)
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- Hypophosphorous acid-iodine: An efficient and mild reagent for cleavage of N-C bond
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A mixture of hypophosphorous acid (H3PO2) and iodine in acetic acid can selectively cleave the N-alkyl bond in a variety of substituted heterocylic compounds in good to excellent yields without any damage to amide bond present in the substrates.
- Meng, Ge,He, Yan-Ping,Chen, Fen-Er
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p. 2593 - 2598
(2007/10/03)
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