- 4-SUBSTITUTED AMINOISOQUINOLINE DERIVATIVES
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[00397] This invention relates to 4-substituted isoquinoline compounds and their derivatives and uses thereof for treatment of cancer, for example, acute myeloid leukemia.
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Paragraph 00277; 00278; 00280
(2018/03/09)
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- Α 7 as intranuclear hydroxynicotinic acetylcholine receptor quinuclidines compd.
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PROBLEM TO BE SOLVED: To provide ligands for the nicotinic α-7 receptor used for the treatment of various disorders of the central nervous system, especially affective and neurodegenerative disorders.SOLUTION: The disclosure provides compounds of the specified formula I, including their salts, and compositions and methods using the compounds.
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Paragraph 0590; 0592
(2018/10/03)
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- Isoquinolin-3-Ylurea Derivatives
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The invention relates to isoquinolin-3-ylurea derivatives of formula (I) wherein R1 represents (C1-C3)alkyl, (C1-C3)haloalkyl or cyclopropyl, R4 represents H and the substituents R2 and R3 and R5 have the meanings disclosed in the specification; and to the salts of such compounds. These compounds are useful for the prevention or the treatment of bacterial infections.
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Paragraph 0698; 0783; 0784; 0785
(2013/04/24)
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- ANTIBACTERIAL ISOQUINOLIN-3-YLUREA DERIVATIVES
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The invention relates to isoquinolin-3-ylurea derivatives of formula (I) wherein R1 represents (C1-C3)alkyl, (C1-C3)haloalkyl or cyclopropyl, R4 represents H and the substituents R2 and R3 and R5 have the meanings disclosed in the specification; and to the salts of such compounds. These compounds are useful for the prevention or the treatment of bacterial infections.
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Page/Page column 108
(2011/10/13)
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- THIADIAZOLE MODULATORS OF PKB
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The invention relates to thiazole compounds of Formula I and Formula II and compositions thereof useful for treating diseases mediated by protein kinase B (PKB) where the variables have the definitions provided herein. The invention also relates to the th
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Page/Page column 188; 189
(2009/03/07)
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- HETEROCYCLIC MODULATORS OF PKB
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The invention relates to heterocyclic compounds of Formula I and compositions thereof useful for treating diseases mediated by protein kinase B (PKB) where the variables have the definitions provided herein Formula (I). The invention also relates to the therapeutic use of such compounds and compositions thereof in treating disease states associated with abnormal cell growth, cancer, inflammation, and metabolic disorders.
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Page/Page column 159-160
(2009/03/07)
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- SUBSTITUTED 2-AMINO-FUSED HETEROCYCLIC COMPOUNDS
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The present invention relates to compounds of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein: R1, R2, Z1, t, and ring A are as defined in the specification. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and methods of treating a condition that is mediated by the modulation of JNK, such as diabetes, the method comprising administering to a mammal an effective amount of a compound of formula (I).
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Page/Page column 17; 36
(2008/06/13)
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- Isoquinoline-pyridine-based protein kinase B/Akt antagonists: SAR and in vivo antitumor activity
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The structure-activity relationships of a series of isoquinoline-pyridine-based protein kinase B/Akt antagonists have been investigated in an effort to improve the major short-comings of the lead compound 3, including poor pharmacokinetic profiles in several species (e.g., mouse iv t1/2 = 0.3 h, po F = 0%). Chlorination at C-1 position of the isoquinoline improved its pharmacokinetic property in mice (iv t1/2 = 5.0 h, po F = 51%) but resulted in >500-fold drop in potency. In a mouse MiaPaCa-2 xenograft model, an amino analog 10y significantly slowed the tumor growth, however was accompanied by toxicity.
- Zhu, Gui-Dong,Gong, Jianchun,Claiborne, Akiyo,Woods, Keith W.,Gandhi, Viraj B.,Thomas, Sheela,Luo, Yan,Liu, Xuesong,Shi, Yan,Guan, Ran,Magnone, Shayna R.,Klinghofer, Vered,Johnson, Eric F.,Bouska, Jennifer,Shoemaker, Alexander,Oleksijew, Anatol,Stoll, Vincent S.,Jong, Ron De,Oltersdorf, Tilman,Li, Qun,Rosenberg, Saul H.,Giranda, Vincent L.
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p. 3150 - 3155
(2007/10/03)
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