- NOVEL TRICYCLIC COMPOUNDS AS ANTICANCER AGENTS
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The present invention is directed to tricyclic compounds, pharmaceutically acceptable compositions comprising compounds of the invention and methods of using said compositions in the treatment of various disorders.
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Paragraph 0980; 0981
(2016/07/27)
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- SULFONAMIDE RETINOIC ACID RECEPTOR-RELATED ORPHAN RECEPTOR MODULATORS AND USES THEREOF
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Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of Retinoic Acid Receptor-Related Orphan Receptor regulated diseases and disorders.
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Paragraph 0257; 0258
(2016/02/16)
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- TRICYCLIC COMPOUNDS AS ANTICANCER AGENTS
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The present invention is directed to tricyclic compounds (I), pharmaceutically acceptable compositions comprising compounds of the invention and methods of using said compositions in the treatment of various disorders.
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Page/Page column 375
(2015/07/15)
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- RETINOIC ACID RECEPTOR-RELATED ORPHAN RECEPTOR MODULATORS AND USES THEREOF
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Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of Retinoic Acid Receptor-Related Orphan Receptor regulated diseases and disorders.
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Paragraph 0218; 0219
(2015/09/28)
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- 1,2,3-triazolium ionic liquids
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The present invention relates to compositions of matter that are ionic liquids, the compositions comprising substituted 1,2,3-triazolium cations combined with any anion. Compositions of the invention should be useful in the separation of gases and, perhap
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Page/Page column 26
(2014/12/12)
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- Probing the structure-property relationship of regioisomeric ionic liquids with click chemistry
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Understanding the structure-property relationship of ionic liquids is a key to the development of optimized materials for specific applications, such as CO2 capture, battery electrolytes, or lubricants. Using Cu(i)-catalyzed click chemistry as
- Nulwala, Hunaid B.,Tang, Chau N.,Kail, Brian W.,Damodaran, Krishnan,Kaur, Palwinder,Wickramanayake, Shan,Shi, Wei,Luebke, David R.
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supporting information; experimental part
p. 3345 - 3349
(2012/02/01)
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- α-Alkyl-α-aminosilanes. 1. Metalation and alkylation between silicon and nitrogen
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tert-Butyl carbamate derivatives of readily available aminomethyltrialkylsilanes have been studied for their ability to undergo metalation between nitrogen and silicon, followed by reaction with an electrophile. Metalation is rapid and reaction with a variety of electrophiles proceeds efficiently. When a benzyl group is attached to nitrogen, benzylic deprotonation competes with deprotonation next to silicon.
- Sieburth, Scott McN.,Somers, Joseph J.,O'Hare, Heather K.
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p. 5669 - 5682
(2007/10/03)
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- Synthesis, Antitumor Activity, and Chemical Properties of Silaplatin and Related Platinum(II) and Platinum(IV) Complexes Derived from β-Silyl Amines
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Platinum(II) and platinum(IV) coordination complexes derived from β-silyl-substituted amines were prepared.The solubility of selected complexes in water and physiological saline was measured, and the effect of the β-silicon on the reactivity of the complex in aqueous solution was determined by HPLC.The stabilities of selected silyl complexes were compared to the carbon analogues.The cyclic complexes 2a ("silaplatin") and its Pt(IV) analogue, 2b, were very active against L1210 leukemia in vivo.Both the platinum(II) complex 2a and the platinum(IV) complex 2b produced a significant number of cures over the dose range 10-40 mg/kg.The platinum(II) complex 2a, silaplatin, was very active in vivo against an L1210 leukemia subline that was resistant to cisplatin; 2a was also active, when given ip against ic implanted L1210.The cyclobutanedicarboxylic acid complex 3c was synthesized; this complex was active against both cisplatin sensistive and resistant L1210 leukemia but was less potent than the analogous dichloro compound 2a.The acyclic platinum(II) and platinum(IV) complexes 1a,b were synthesized and unexpectedly found to be inactive in vivo against L1210 leukemia.More lipophilic silaplatin analogues were prepared-Pt(II) complex 2c and Pt(IV) complex 2d have one additional methylene carbon compared to 2a,b, whereas Pt(II) complex 2e and Pt(IV) complex 2f have two additional methylene carbons.Cyclization of the alkyl groups attached to the silicon gave the spiro bicyclic Pt(II) complexes 10a and 11a and the Pt(IV) complexes 10 b and 11b.
- Anderson, Wayne K.,Kasliwal, Ravindra,Houston, D. Michael,Wang, Yueh-sha,Narayanan, Ven L.,et al.
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p. 3789 - 3797
(2007/10/03)
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- The Synthesis of Pyrroles with Insecticidal Activity
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The 2-aryl-4-bromo-5-trifluoromethylpyrrole-3-carbonitriles represent a new class of insect control agents. The high insecticidal activity observed in this series prompted us to investigate the preparation of regioisomeric arylhalotrifluoromethylpyrrole c
- Kuhn, David G.,Kamhi, Victor M.,Furch, Joseph A.,Diehl, Robert E.,Lowen, Gregory T.,Kameswaran, Venkataraman
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p. 279 - 286
(2007/10/03)
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- Platinum complexes derived from b-silyamines
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This invention relates to new cis diamino platinum complexes; to compositions comprising these complexes; and to processes for their utility as fungicides, bacteriocides and as inhibitors of the growth of cancer in warm-blooded animals, wherein the comple
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- Synthesis of 3,9b-Dihydro-5H-pyrroloisoindoles and 3,5,6,10b-Tetrahydropyrroloisoquinolines with 1,3-Dipolar Cycloaddition Reactions.
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The title classes of compounds have been prepared using a sequence of two ring-forming reactions.Initial 1,3-dipolar cycloaddition with an azomethine ylide gave N-acylated 3-pyrrolines which were further elaborated to the target compounds by a tandem deprotection/cyclization reaction.
- Anderson, Wayne K.,Kinder, Frederick R.
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p. 975 - 979
(2007/10/02)
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- Synthesis and Antineoplastic Activity of Bisoxy>methyl>-Substituted 3-Pyrrolines as Prodrugs of Tumor Inhibitory Pyrrole Bis(carbamates)
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A series of bispyrrolines 2-4 were synthesized from either the appropriate α-silylated iminium salt, or an aziridine, or a 2H-azirine in a sequence involving 1,3-dipolar cycloaddition reactions.The antineoplastic activities of the pyrrolines were compared to the corresponding pyrroles.The C-2 gem-dimethyl-substituted pyrroline, 4, which cannot be converted to the pyrrole in vivo, was inactive.The activity of the 2-phenyl-substituted pyrrolines 3 was markedly dependent on the nature of the phenyl substituent, although the correspondingphenylpyrroles all showed comparable activity.The differences in the activities of the pyrrolines 3 may be due to the rate of metabolic conversion of the pyrroline to the pyrrole.Electron-withdrawing substituents on the phenyl ring appear to retard this process.
- Anderson, Wayne K.,Milowsky, Arnold S.
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p. 2241 - 2249
(2007/10/02)
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- Synthesis and Reactions of Trimethylsilylmethyl Azide
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Trimethylsilylmethyl azide, prepared quantitatively from trimethylsilylmethyl chloride and sodium azide, could be used for the amination of aryl Grignard reagents or aryl-lithium compounds.
- Nishiyama, Kozaburo,Tanaka, Nobuko
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p. 1322 - 1323
(2007/10/02)
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- A SILYL-FUNCTIONALIZED ALKYL AZIDE, TRIMETHYLSILYLMETHYL AZIDE; SYNTHESIS AND CYCLOADDITION REACTION TO ACETYLENIC DIPOLAROPHILES
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Thermally stable trimethylsilylmethyl azide was first synthesized from the reaction of chloromethyltrimethylsilane with sodium azide.Its use as an α-functionalized synthetic equivalent of methyl azide was demonstrated in the reaction with acetylenic dipol
- Tsuge, Otohiko,Kanemasa, Shuji,Matsuda, Koyo
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p. 1131 - 1134
(2007/10/02)
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