- Solid dispersions containing an apoptosis-inducing agent
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A pro-apoptotic solid dispersion comprises, in essentially non-crystalline form, a Bcl-2 family protein inhibitory compound of Formula I as defined herein, dispersed in a solid matrix that comprises (a) a pharmaceutically acceptable water-soluble polymeric carrier and (b) a pharmaceutically acceptable surfactant. A process for preparing such a solid dispersion comprises dissolving the compound, the polymeric carrier and the surfactant in a suitable solvent, and removing the solvent to provide a solid matrix comprising the polymeric carrier and the surfactant and having the compound dispersed in essentially non-crystalline form therein. The solid dispersion is suitable for oral administration to a subject in need thereof for treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer.
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Page/Page column 169
(2019/03/15)
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- Substituted imidazo[1,2-b]pyridazines as protein kinase inhibitors
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The present invention provides protein kinase having one of the following structures (I), (II) or (III): or a stereoisomer, prodrug, tautomer or pharmaceutically acceptable salt thereof, wherein R, R1, R2 and X are as defined herein. Compositions and methods for using the same in the treatment of cancer, autoimmune, inflammatory and other Pim kinase-associated conditions are also disclosed.
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- HETEROCYCLIC PROTEIN KINASE INHIBITORS
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The present invention provides protein kinase having one of the following structures (I), (II) or (III): or a stereoisomer, prodrug, tautomer or pharmaceutically acceptable salt thereof, wherein R, R1, R2 and X are as defined herein. Compositions and methods for using the same in the treatment of cancer, autoimmune, inflammatory and other Pim kinase-associated conditions are also disclosed.
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- SUBSTITUTED ISOINDOLONES AND THEIR USE AS METABOTROPIC GLUTAMATE RECEPTOR POTENTIATORS
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The present invention is directed to compounds of formula I: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 and n are as defined for formula I in the description. The invention also relates to processes for the preparation of the compounds and to new intermediates employed in the preparation, pharmaceutical compositions containing the compounds, and to the use of the compounds in therapy.
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Page/Page column 18
(2009/05/29)
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- 4-Amino-2-cyanopyrimidines: Novel scaffold for nonpeptidic cathepsin S inhibitors
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We describe here a novel 4-amino-2-cyanopyrimidine scaffold for nonpeptidomimetic cathepsin S selective inhibitors. Some of the synthesized compounds have sub-nanomolar potency and high selectivity toward cathepsin S along with promising pharmacokinetic a
- Irie, Osamu,Yokokawa, Fumiaki,Ehara, Takeru,Iwasaki, Atsuko,Iwaki, Yuki,Hitomi, Yuko,Konishi, Kazuhide,Kishida, Masashi,Toyao, Atsushi,Masuya, Keiichi,Gunji, Hiroki,Sakaki, Junichi,Iwasaki, Genji,Hirao, Hajime,Kanazawa, Takanori,Tanabe, Keiko,Kosaka, Takatoshi,Hart, Terance W.,Hallett, Allan
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scheme or table
p. 4642 - 4646
(2009/04/06)
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- A PROCESS FOR PRODUCING [(4,4- DIF LUOROCYCLOHEXYL) METHYL] AMINE
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A process for preparing a compound of formula I wherein R1 is H, C1-6alkyl, C2-6alkenyl, C1-6alkoxy, -OH, or amino; and n, m, and p are independently selected from 0, 1 and 2; which process comprises reacting a
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Page/Page column 11-12
(2008/06/13)
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- SUBSTITUTED ISOINDOLONES AND THEIR USE AS METABOTROPIC GLUTAMATE RECEPTOR POTENTIATORS
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The present invention is directed to compounds of formula (I), wherein R1 is a ring, R5 is a specified substituent, and n is from 1 to 8. The invention also relates to the use of the compounds in therapy as metabotropic glutamate receptors modulators, particularly in neurological and psychiatric disorders.
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Page/Page column 35
(2010/11/26)
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- PROCESS FOR THE PREPARATION OF GEMINAL ((DIFLUOROCYCLOALKYL)METHYL) AMINES.
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The present invention relates to a process of preparing a compound of formula II, wherein R1, n, m and p are defined in the specification.
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Page/Page column 10
(2008/06/13)
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- Substituted benzothiazole amide derivatives
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A compound of formula I and a method of treatment of diseases, related to modulation of the adenosine A2 receptor system comprising administering a compound of formula 1to a person in need of such treatment.
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