- AURORA AND FLT3 KINASES MODULATORS
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The invention provides a compound having the formula (1): and salts thereof; wherein: R1 is hydrogen or C1-2 alkyl; and R2, R3 and R4 are the same or different and each is selected from hydrogen, C1-2 alkyl, fluorine, chlorine, C1-2 alkoxy and trifluoromethyl, provided that no more than two of R2, R3 and R4 are other than hydrogen. Also provided are pharmaceutical compositions containing the compounds and their use in medicine, and in particular in the treatment of cancer.
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Paragraph 0185; 0186
(2015/02/18)
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- AURORA AND FLT3 KINASES MODULATORS
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The invention provides a compound having the formula (1) useful as modulator of the activity of Aurora kinases and FLT3 kinases: and salts thereof; wherein: R1 is hydrogen or C1-2 alkyl; and R2, R3 and R4 are the same or different and each is selected from hydrogen, C1-2 alkyl, fluorine, chlorine, C1-2 alkoxy and trifluoromethyl, provided that no more than two of R2, R3 and R4 are other than hydrogen. Also provided are pharmaceutical compositions containing the compounds and their use in medicine, and in particular in the treatment of cancer
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Page/Page column 41-42
(2013/08/28)
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- TETRACYCLIC XANTHENE DERIVATIVES AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES
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The present invention relates to novel Tetracyclic Xanthene Derivatives of Formula (I) and pharmaceutically acceptable salts thereof, wherein A, Y1, Y2, Z, Ra, Rb, R1a, R1b and R2 are as defined herein. The present invention also relates to compositions comprising at least one Tetracyclic Xanthene Derivative, and methods of using the Tetracyclic Xanthene Derivatives for treating or preventing HCV infection in a patient.
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- TETRACYCLIC XANTHENE DERIVATIVES AND METHODS OF USE THEREOF FOR TREATMENT OF VIRAL DISEASES
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The present invention discloses tetracyclic xanthene derivatives of Formula (I) and pharmaceutically acceptable salts thereof, wherein A, Y1, Y2, Z, Ra, Rb, R1a, R1b, and R2 are as defined herein. The present invention also discloses compositions comprising at least one tetracyclic xanthene derivative, and methods of using the tetracyclic xanthene derivatives for treating or preventing HCV infection in a patient.
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- Synthetic studies on dragmacidin D: Synthesis and assembly of three fragments towards an advanced intermediate
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We report herein the approach to the key advanced intermediate in the synthesis of the bioactive marine natural product dragmacidin D. By employing a modular synthesis strategy of three fragments (5, 7, and 8), the advanced intermediate 3 has been successfully synthesized in 2.5% yield over 15 steps by starting from nitrotoluene 20. The synthesis also involves sequential cross-coupling reactions, namely Sonogashira and Suzuki-Miyaura reactions, so that various analogues can be efficiently synthesized, which will allow the study of structure-activity relationships of dragmacidin D.
- Oikawa, Masato,Ikoma, Minoru,Sasaki, Makoto
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p. 4654 - 4666
(2011/10/03)
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- INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION
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Compounds of formula (I): wherein R4, R6 and R7 are defined herein, are useful as inhibitors of HIV replication.
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Page/Page column 111
(2009/06/27)
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- INDOLES AS 5-HT6 MODULATORS
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The present invention relates to novel compounds of formula (I) wherein m, n, R0, R1, R2, R3 and R4 are as described herein, to pharmaceutical compositions comprising the compounds, to processes for t
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Page/Page column 100
(2008/06/13)
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- Synthetic studies on dragmacidin D: synthesis of the left-hand fragment
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We report a synthesis of a left-hand fragment of bis(indole)-class marine alkaloid, dragmacidin D. The synthesis features Suzuki-Miyaura reaction for the coupling of imidazolyl boronic acid and (4-indolyl)vinyl bromide.
- Ikoma, Minoru,Oikawa, Masato,Sasaki, Makoto
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scheme or table
p. 7197 - 7199
(2009/04/11)
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- 3-Amino-1-arylpropyl indoles and aza-substituted indoles and uses thereof
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The present invention provides compounds of the formula: or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein p, Ar, R1, R2, R3, Ra, Rb, Rc, Rd and Re are defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds.
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Page/Page column 67-68
(2008/06/13)
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- Enantioselective synthesis of the aminoimidazole segment of dragmacidin D
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A facile enantioselective synthesis of the 2-aminoimidazole side-chain of dragmacidin D has been developed, which involved the regio- and stereoselective opening of the chiral epoxide 9 by a diindolylcuprate reagent, followed by further steps to give 5-substituted N-(1H-imidazol-2-yl)acetamide 2.
- Yang, Cai-Guang,Wang, Jun,Jiang, Biao
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p. 1063 - 1066
(2007/10/03)
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