- IRAK INHIBITORS AND METHOD FOR MAKING AND USING
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Disclosed embodiments concern interleukin receptor associated kinases (IRAK) inhibitors, such as oxazole compounds, and compositions comprising such inhibitors. Also disclosed are methods of making and using the compounds and compositions. The disclosed c
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Paragraph 0377-0379
(2018/05/03)
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- AMIDE COMPOUNDS AND METHOD FOR MAKING AND USING
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Disclosed embodiments concern novel interleukin receptor associated kinases (IRAK) inhibitors and compositions comprising such inhibitors. Also disclosed are methods of making and using the compounds and compositions. The disclosed compounds and/or compos
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Paragraph 0656-0658
(2018/05/03)
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- Thermoresponsive star-like γ-substituted poly(caprolactone)s for micellar drug delivery
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Temperature responsive drug carriers are attractive due to their ability to provide controlled release of the encapsulated cargo based on the use of external stimuli. In this work, 4- and 6-arm thermoresponsive star-like block copolymers were synthesized
- Washington, Katherine E.,Kularatne, Ruvanthi N.,Du, Jia,Ren, Yixin,Gillings, Matthew J.,Geng, Calvin X.,Biewer, Michael C.,Stefan, Mihaela C.
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p. 5632 - 5640
(2017/07/25)
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- PIPERAZINE DERIVATIVES AS HIV PROTEASE INHIBITORS
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The present invention is directed to compounds of Formula I pharmaceutical compositions comprising the same, and their use in the inhibition of HIV protease, the inhibition of HIV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS.
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Page/Page column 89
(2015/10/05)
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- A combined experimental and computational study of the substituent effect on micellar behavior of γ-substituted thermoresponsive amphiphilic poly(ε-caprolactone)s
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The effect of the core substituent structure on the micellar behavior of thermoresponsive amphiphilic poly(ε-caprolactone) diblock copolymer micelles was investigated through a combination of experimental and computational methods. The polycaprolactone (P
- Hao, Jing,Cheng, Yixing,Ranatunga, R. J. K. Udayana,Senevirathne, Suchithra,Biewer, Michael C.,Nielsen, Steven O.,Wang, Qian,Stefan, Mihaela C.
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p. 4829 - 4838
(2013/07/26)
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- CYCLOHEXYL-AZETIDINYL ANTAGONISTS OF CCR2
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The present invention comprises compounds of Formula (I). wherein: R1, R2, X, and Z are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).
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Page/Page column 64
(2012/01/03)
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- 1- (1-CYCLOHEXYL-4-PIPERIDINYL) -1, 3-DIHYDRO-2H-BENZIMIDAZOL-2-ONE DERIVATIVES WHICH HAVE ACTIVITY ON THE M1 RECEPTOR AND THEIR USE IN MEDICINE
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Compounds of formula (I) or a salt thereof are provided, wherein X1, X2, X3, R6, Q and R are as defined in the description. Uses of the compounds as medicaments and in the manufacture of medicaments for treating
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Page/Page column 56-57
(2008/12/04)
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- BENZIMIDAZOLES WHICH HAVE ACTIVITY AT M1 RECEPTOR AND THEIR USES IN MEDICINE
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Compounds of formula (I), salts and solvates are provided: formula (I), wherein Q, R and R6 are as defined in the claims. Uses of the compounds for therapy, for example in the treatment of psychotic disorders and cognitive impairment, are also disclosed.
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Page/Page column 52
(2008/06/13)
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- BENZIMIDAZOLES WHICH HAVE ACTIVITY AT M1 RECEPTOR AND THEIR USES IN MEDICINE
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Compounds of Formula (I) and salts and solvates are provided; wherein R, R5, R6 and Q are defined as in the claims. Uses of the compounds for therapy, for example in the treatment of psychotic disorders and cognitive impairment, are also disclosed.
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Page/Page column 53
(2010/11/28)
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- New bioorganic reagents: Evolved cyclohexanone monooxygenase - Why is it more selective?
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Four mutants of the cyclohexanone monooxygenase (CHMO) evolved as catalysts for Baeyer-Villiger oxidation of 4-hydroxycyclohexanone were investigated as catalysts for a variety of 4-substituted and 4,4-disubstituted cyclohexanones. Several excellent catalytic matches (mutant/substrate) were identified. The most important, however, is the finding that, in a number of cases, a mutant with a single exchange, Phe432Ser, was shown to be as robust and more selective as a catalyst than the wild-type CHMO. All biotransformations were performed on a laboratory scale, allowing full characterization of the products. The absolute configurations of two products were established. A model suggesting a possible role of the 432 serine residue in enantioselectivity control is proposed.
- Kayser, Margaret M.,Clouthier, Christopher M.
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p. 8424 - 8430
(2007/10/03)
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- Direct evidence for anchimeric assistance in alcohol elimination from gas-phase MH+ ions of 1,4-dialkoxycyclohexanes under chemical ionisation. Experiment and theory
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trans-1,4-Dialkoxycyclohexanes afford very abundant [MH - ROH]+ ions upon chemical ionisation (CI), in contrast to the cis-isomers, suggesting anchimeric assistance in the alcohol elimination from the MH+ ions of the trans-diethers. Collision induced dissociation (CID) measurements of the [MH - ROH]+ ions, obtained from various suitably deuterium labelled stereoisomeric 1-ethoxy-4-methoxycyclohexanes, indicated fromation of symmetrical bicyclic ethyl and methyl oxonium ions by an anchimerically assisted alcohol elimination from the trans-diethers. On the other hand these measurements suggest that the cis-isomers afford isomeric monocyclic O-protonated 4-alkoxycyclohexene cations, in which the hydrogens at positions 2 and 3 (as well as those at positions 5 and 6, and 1 and 4) are not equivalent. The two results, namely the symmetrical bicyclic structure and the high abundance of the [MH - ROH]+ ions in the CI mass spectra of the trans-diethers, in contrast to the non-symmetrical monocyclic structure and low abundance of these ions in the cis-isomers, are suggested to be direct evidence for anchimeric assistance in a gas-phase ion dissociation process. Ab initio calculations at the MP3/6-31G*//6-31G* level support the anchimerically assisted elimination mechanism observed in trans-1-ethoxy-4-methoxycyclohexane, but also show that the energy difference between the anchimerically assisted and non-assisted elimination mechanisms is small (ca. 2-3 kcal mol-1)(1 cal = 4.184 J).
- Shvily, Ronit,Mueller, Thomas,Apeloig, Yitzhak,Mandelbaum, Asher
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p. 1221 - 1234
(2007/10/03)
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