- INHIBITORS OF LIN28 AND METHODS OF USE THEREOF
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The present disclosure relates to compounds of formula (I) and compositions comprising the same. The disclosure further relates to methods of treating cancers.
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Page/Page column 52; 63-64; 97
(2021/06/26)
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- Compounds for treating spinal muscular atrophy
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Provided herein are compounds, compositions thereof and uses therewith for treating spinal muscular atrophy. In a specific embodiment, provided herein are compounds of a form that may be used to modulate the inclusion of exon 7 of SMN2 into mRNA that is transcribed from the SMN2 gene. In another specific embodiment, provided herein are compounds of a form that may be used to modulate the inclusion of exon 7 of SMN1 into mRNA that is transcribed from the SMN1 gene. In yet another embodiment, provided herein are compounds of a form that may be used to modulate the inclusion of exon 7 of SMN1 and SMN2 into mRNA that is transcribed from the SMN1 and SMN2 genes, respectively.
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Page/Page column 409; 410
(2017/05/02)
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- IMIDAZOPYRIDAZINE DERIVATIVES AS ΡΙ3Κβ INHIBITORS
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The present invention relates to substituted imidazopyridazine derivatives of Formula (I) wherein the variables have the meaning defined in the claims. The compounds according to the present invention are useful as pΙ3Κβ inhibitors. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
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Page/Page column 113
(2016/07/05)
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- Combination of mTOR inhibitors and P13-kinase inhibitors, and uses thereof
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The present invention provides for a method for treating a disease condition associated with PI3-kinase α and/or mTOR in a subject. In another aspect, the invention provides for a method for treating a disease condition associated with PI3-kinase α and/or mTOR in a subject. In yet another aspect, a method of inhibiting phosphorylation of both Akt (S473) and Akt (T308) in a cell is set forth.
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Page/Page column 348
(2016/04/26)
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- COMBINATION OF KINASE INHIBITORS AND USES THEREOF
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The present invention provides for a method for treating a disease condition associated with PI3-kinase a and/or a receptor tyrosine kinase (RTK) in a subject. In another aspect, the invention provides for a method for treating a disease condition associated with PI3-kinase α and/or an RTK in a subject. In yet another aspect, a method of inhibiting phosphorylation of Akt (S473) in a cell is set forth.
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Page/Page column 69
(2015/02/19)
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- TRIAZOLO COMPOUNDS
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The present invention relates to compounds of formula (I) and its use for the treatment of neurological disorders.
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Page/Page column 30; 52
(2014/05/24)
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- MIXED LINEAGE KINASE INHIBITORS AND METHOD OF TREATMENTS
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Provided herein are imidazopyridine compounds having an inhibitory effect on mixed lineage kinases (MLKs), methods of their synthesis, and methods of their therapeutic. Also provided are pharmaceutical compositions comprising the compounds and methods of
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Paragraph 0266-0268
(2014/09/29)
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- COMBINATION OF KINASE INHIBITORS AND USES THEREOF
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The present invention provides for a method for treating a disease condition associated with PI3-kinase a and/or mTOR in a subject. In another aspect, the invention provides for a method for treating a disease condition associated with PI3-kinase a and/or mTOR in a subject. In yet another aspect, a method of inhibiting phosphorylation of both Akt (S473) and Akt (T308) in a cell is set forth. The present invention also provides a pharmaceutical kit effective for treating a disease condition associated with PI3 -kinase α and/or mTOR in a subject.
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Paragraph 00641
(2014/10/04)
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- Development of an alternate synthesis for a key JAK2 inhibitor intermediate via sequential c-h bond functionalization
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The development of an alternative synthetic route to a functionalized imidazopyridazine which strategically streamlines the synthesis and avoids a number of problematic reagents is described. Key to the success of this alternative route is the use of two
- Campbell, Alison N.,Cole, Kevin P.,Martinelli, Joseph R.,May, Scott A.,Mitchell, David,Pollock, Patrick M.,Sullivan, Kevin A.
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p. 273 - 281
(2013/04/10)
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- IMIDAZOPYRIDAZINES FOR USE AS PROTEIN KINASE INHIBITORS
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There is provided compounds of formula (I): wherein Z, M, R1, X, R3, R4 and R5 have meanings given in the description, an pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protei kinase (e.g. a PIM family kinase or PI3-K) is desired and/or required, an particularly in the treatment of cancer.
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Page/Page column 103
(2009/06/27)
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- SUBSTITUTED IMIDAZOPYRIDAZINES AS PI3K LIPID KINASE INHIBITORS
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The invention relates to novel compounds of formula (I), as well as other invention embodiments related to these compounds. The compounds are e.g. useful in the treatment of the animal or human body in view of their ability to inhibit protein kinases such as especially PI3 kinase.
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Page/Page column 81
(2009/01/20)
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- Synthesis of imidazo[1,2-b]pyridazines: Fenbendazole, oxifenbendazole analogs and related derivatives
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A series of imidazo[1,2-b]pyridazines has been prepared and evaluated for macrofilaricidal activity against Brugia pahangi or Acanthocheilonema viteae infections in jirds. The imidazo[1,2-b]pyridazine analogs of fenbendazole and oxifenbendazole are report
- Mourad,Wise,Townsend
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p. 1365 - 1372
(2007/10/02)
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