- Ansa-Zirconocene Catalysts for Isotactic-Selective Propene Polymerization at High Temperature: A Long Story Finds a Happy Ending
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Absolute rigidity is rare in the "soft"world of organometallics. Here we introduce two cyclopenta[a]triptycyl ansa-zirconocene catalysts for isotactic-selective propene polymerization, designed by means of an integrated high-throughput experimentation/qua
- Kulyabin, Pavel S.,Goryunov, Georgy P.,Sharikov, Mikhail I.,Izmer, Vyatcheslav V.,Vittoria, Antonio,Budzelaar, Peter H. M.,Busico, Vincenzo,Voskoboynikov, Alexander Z.,Ehm, Christian,Cipullo, Roberta,Uborsky, Dmitry V.
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- HETEROCYCLIC COMPOUND AND USE THEREOF
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The present invention provides a heterocyclic compound having an orexin type 2 receptor agonist activity. A compound represented by the formula (I) : wherein each symbol is as described in the specification, or a salt thereof, is useful as an agent for the prophylaxis treatment of narcolepsy.
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Paragraph 0356
(2019/02/15)
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- Nitrile in the Hole: Discovery of a Small Auxiliary Pocket in Neuronal Nitric Oxide Synthase Leading to the Development of Potent and Selective 2-Aminoquinoline Inhibitors
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Neuronal nitric oxide synthase (nNOS) inhibition is a promising strategy to treat neurodegenerative disorders, but the development of nNOS inhibitors is often hindered by poor pharmacokinetics. We previously developed a class of membrane-permeable 2-amino
- Cinelli, Maris A.,Li, Huiying,Chreifi, Georges,Poulos, Thomas L.,Silverman, Richard B.
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supporting information
p. 3958 - 3978
(2017/05/19)
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- Substituted 1-benzylcycloalkylcarboxylic acids and the use thereof
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The present application relates to novel substituted 1-benzylcycloalkylcarboxylic acid derivatives, to processes for their preparation, to their use for the treatment and/or prevention of diseases, and to their use for producing medicaments for the treatment and/or prevention of diseases, especially for the treatment and/or prevention of cardiovascular disorders.
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Page/Page column 19-20
(2012/07/14)
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- OXO-HETEROCYCLIC SUBSTITUTED CARBOXYLIC ACID DERIVATIVES AND THE USE THEREOF
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The present application relates to novel carboxylic acid derivatives having an oxo-substituted azaheterocyclic partial structure, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for producing medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prevention of cardiovascular disorders.
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Page/Page column 96
(2011/02/26)
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- HETEROCYCLYL PYRAZOLOPYRIMIDINE ANALOGUES AS JAK INHIBITORS
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The present invention relates to compounds of formula (I) wherein X1 to X5, Y, Z1 to Z3, and R have the meaning as cited in the description and the claims. Said compounds are useful as JAK inhibitors for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immunologically-mediated diseases. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments.
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Page/Page column 214; 220; 221; 223; 224
(2011/05/06)
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- Discovery of selective metal-binding peptoids using 19F encoded combinatorial libraries
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A method for encoding solid-phase split/mix combinatorial libraries using the chemical shift of synthetic fluoroarenes ('F-codes') has been developed. They have wide chemical shift dispersion and are detectable at the sub-μmol level. 19F NMR is
- Pirrung, Michael C.,Park, Kaapjoo
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p. 2115 - 2118
(2007/10/03)
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- 3,4-dihydro-4-oxo-3-(2-propenyl)-1-phthalazineacetic acids and derivatives, their preparations and medicines containing them
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Novel 3,4-dihydro-4-oxo-3(prop-2-enyl)-1-phtalazineacetic acids and derivatives of formula (I) STR1 in which R1 R2 and R3 are the same or different and stand for H, a halogen or a linear or branched aliphatic, saturated or unsaturated radical, substituted or not by at least one halogen or R4 residue such as defined below, except when R4 is H; R4 and R5 are the same or different and stand for H, a linear or branched aliphatic radical, saturated or unsaturated, an aryl or heteroaryl radical, said radicals being substituted or not by at least one grouping such as fluorine, chlorine, bromine, methyl or trifluoromethyl, where R4 and R5 do not simultaneously denote H; R6 stands for hydroxy or alkoxy radical; R7 stands for H, a halogen, a linear or branched aliphatic saturated or unsaturated radical, an alkoxy radical, said radicals being substituted or not by analiphatic or halogenated radical, a nitro group, a substituted or unsubstituted amino group, S(O)n R8 or a cyano group; n is equal to 0,1 or 2; R8 is an aliphatic, linear or branched radical, an aryl or heteroaryl radical, an amino radical, said radicals being substituted or not by an aliphatic or halogenated radical. This invention also relates to the optional tautomeric forms of said acids and their pharmaceutically acceptable base addition salts. Also described is a process for preparing said compounds and the drugs containing same.
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