- Discovery of DS34942424: An orally potent analgesic without mu opioid receptor agonist activity
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We identified (5′S)-10′-fluoro-6′-methyl-5′,6′-dihydro-3′H-spiro[cyclopropane-1,4′-[2,6]diaza[2,5]methano[2,6]benzodiazonin]-7′(1′H)-one, 22b (DS34942424) with a unique and original bicyclic skeleton. 22b showed an orally potent analgesic in the acetic ac
- Arita, Tsuyoshi,Asano, Masayoshi,Domon, Yuki,Kubota, Kazufumi,Machinaga, Nobuo,Shimada, Kousei
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- BENZAMIDE DERIVATIVE
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The present invention relates to benzamide derivatives represented by formula (I) or pharmaceutically acceptable salts thereof.
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Paragraph 1593
(2015/03/16)
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- QUINAZOLINEDIONE DERIVATIVE
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The present invention relates to quinazolinedione derivatives represented by formula (I) or pharmaceutically acceptable salts thereof.
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Paragraph 1681
(2015/03/16)
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- Discovery of aminopiperidine-based Smac mimetics as IAP antagonists
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A series of structurally unique Smac mimetics that act as antagonists of inhibitor of apoptosis proteins (IAPs) has been discovered. While most previously described Smac mimetics contain the proline ring (or a similar cyclic motif) found in Smac, a key feature of the compounds described herein is that this ring has been removed. Despite this, compounds in this series potently bind to cIAP1 and elicit the expected phenotype of cIAP1 inhibition in cancer cells. Marked selectivity for cIAP1 over XIAP is observed for these compounds, which is attributed to a slight difference in the binding groove between the two proteins and the resulting steric interactions with the inhibitors. XIAP binding can be improved by constraining the inhibitor so that these unfavorable steric interactions are minimized.
- Hennessy, Edward J.,Saeh, Jamal C.,Sha, Li,MacIntyre, Terry,Wang, Haiyun,Larsen, Nicholas A.,Aquila, Brian M.,Ferguson, Andrew D.,Laing, Naomi M.,Omer, Charles A.
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supporting information; experimental part
p. 1690 - 1694
(2012/04/10)
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- HETEROCYCLIC TYROSINE KINASE INHIBITORS
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The present invention provides compounds useful as inhibitors of Tec family kinases, compositions thereof, and methods of using the same. In certain embodiments, the present invention provides pharmaceutical formulations comprising provided compounds. In certain embodiments, the present invention provides a method of decreasing enzymatic activity of a Tec kinase family member. In some embodiments, such methods include contacting a Tec kinase family member with an effective amount of a Tec kinase family member inhibitor. In certain embodiments, the present invention provides a method of treating a disorder responsive to Tec kinase family inhibition in a subject in need thereof.
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Page/Page column 103-104
(2012/05/19)
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- THERAPEUTIC ISOXAZOLE COMPOUNDS
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The invention provides a compound of formula I: wherein A1, A2, A3, R1, X, Y, and B have any of the values described herein, as well as salts of such compounds, compositions comprising such compounds, and therapeutic methods that comprise the administration of such compounds. The compounds are inhibitors of monoamine oxidase B (MAO-B) enzyme function and are useful for improving cognitive function and for treating psychiatric disorders in animals.
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Page/Page column 44
(2009/04/24)
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- AMIDE DERIVATIVE
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The present invention relates to a compound of the formula (I) being useful as a renin inhibitor, or a pharmaceutically acceptable salt thereof. wherein R1a is a hydrogen atom, an optionally substituted C1-6 alkyl, etc.; R1b is an optionally substituted C1-6 alkoxy, etc.; R1c is a hydrogen atom, an optionally substituted C1-6 alkoxy, etc.; R2 is a hydrogen atom, an optionally substituted C1-6 alkyl, etc.; R3a, R3b, R3c and R3d are independently the same or different, and each is a group of the formula: -A-B (in which A is a single bond, -(CH2)sO-, - (CH2)sN(R4)CO-, etc., B is a hydrogen atom, an optionally substituted C1-6 alkyl, etc.), etc.; R4 is a hydrogen atom, an optionally substituted C1-6 alkyl, etc.; s is 0, etc.; and n is 1, etc.
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Page/Page column 110
(2009/12/05)
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- AMIDO COMPOUNDS AND THEIR USE AS PHARMACEUTICALS
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The present invention relates to inhibitors of 11-β hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-β hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.
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Example 237.1
(2008/06/13)
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