- Prodrugs of compounds that enhance antifungal activity and compositions of said prodrugs
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The invention relates to prodrugs for use in the inhibition of histone deacetylase. The prodrugs of the present invention have good aqueous solubility and good aqueous stability. The prodrugs of the invention advantageously are metabolized to the active i
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Page/Page column 139; 140
(2017/05/17)
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- JANUS KINASES INHIBITORS, COMPOSITIONS THEREOF AND USE THEREOF
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Compounds of Formula (00A) and salts thereof, wherein R1, R2 R3, R4 and n are defined herein, are useful as inhibitors of one or more Janus kinases. Also provided are pharmaceutical compositions that include a compound of Formula (00A) and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of a Janus kinase activity in a patient. ( 00A)
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- Prodrugs of Compounds that Enhance Antifungal Activity and Compositions of Said Prodrugs
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The invention relates to prodrugs for use in the inhibition of histone deacetylase. The prodrugs of the present invention have good aqueous solubility and good aqueous stability. The prodrugs of the invention advantageously are metabolized to the active i
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Paragraph 0436
(2015/07/27)
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- BETA-LACTAMASE INHIBITORS
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Described herein are compounds and compositions that modulate the activity of beta-lactamases. In some embodiments, the compounds described herein inhibit beta-lactamase. In certain embodiments, the compounds described herein are useful in the treatment of bacterial infections.
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- 2-Arylbenzoxazoles as CETP inhibitors: Raising HDL-C in cynoCETP transgenic mice
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We describe structure-activity studies leading to the discovery of 2-arylbenzoxazole 3, the first in a series to raise serum high-density lipoprotein cholesterol levels in transgenic mice. Replacement of the 4-piperidinyloxy moiety with piperazinyl provid
- Kallashi, Florida,Kim, Dooseop,Kowalchick, Jennifer,Park, You Jung,Hunt, Julianne A.,Ali, Amjad,Smith, Cameron J.,Hammond, Milton L.,Pivnichny, James V.,Tong, Xinchun,Xu, Suoyu S.,Anderson, Matt S.,Chen, Ying,Eveland, Suzanne S.,Guo, Qiu,Hyland, Sheryl A.,Milot, Denise P.,Cumiskey, Anne-Marie,Latham, Melanie,Peterson, Laurence B.,Rosa, Raymond,Sparrow, Carl P.,Wright, Samuel D.,Sinclair, Peter J.
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scheme or table
p. 558 - 561
(2011/03/17)
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- GPCR AGONISTS
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Compounds of formula (I): or pharmaceutically acceptable salts thereof, are GPCR agonists and are useful as for the treatment of obesity and diabetes.
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Page/Page column 22
(2010/11/25)
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- CETP INHIBITORS
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Compounds of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. I
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Page/Page column 40
(2008/06/13)
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- HETEROCYCLIC DERIVATIVES AS GPCR RECEPTOR AGONISTS
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Compounds of Formula (I), R1-A-V-B-R2; or pharmaceutically acceptable salts thereof, are agonists of GPR116 and are useful as regulators of satiety, e.g. for the treatment of obesity, and for the treatment of diabetes.
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Page/Page column 23-24
(2008/06/13)
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- Compounds with growth hormone releasing properties
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Compounds of peptide mimetic nature having the general formula I STR1 wherein a and b are independently 1 or 2, R1 and R2 are independently H or C1-6 alkyl, G and J are independently, inter alia, aromats, and D and E are independently several different groups are growth hormone secretagogous with improved bioavailability.
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- Synthesis and in vitro characterization of new growth hormone secretagogues derived from ipamorelin with dipeptidomimetic N-terminals
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The structural requirements for N-terminal features for the minimal structure of growth hormone secretagogues derived from ipamorelin are investigated. It is found, that incorporation of nonpolar peptidomimetic amino acids at the N-terminal can replace the Aib-His moiety and lead to compounds with high in vitro potency with respect to their growth hormone secretagogue properties. New unnatural amino acids with double bonds, ether- linkages, and 1,3-phenylene-moieties in the backbone proved to be valuable dipeptidomimetics. Using them, growth hormone secretagogues with high potencies were obtained.
- Peschke, Bernd,Ankersen, Michael,Sehested Hansen, Birgit,Kruse Hansen, Thomas,Langeland Johansen, Nils,Lau, Jesper,Madsen, Kjeld,Petersen, Hans,Thogersen, Henning,Watson, Brett
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p. 363 - 380
(2007/10/03)
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- Certain diacyl hydrazine derivatives
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The invention concerns acid derivatives of formula I and pharmaceutically acceptable metabolically labile esters or amides thereof, and pharmaceutically acceptable salts thereof, in which R1, R2, R3, X1, Q, X2 and G have the meanings given in the specification. The invention also concerns processes for the preparation of the acid derivatives of formula I, pharmaceutical compositions containing them and their use as inhibitors of the binding of fibrinogen to glycoprotein IIb/IIIa.
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