- Nitrile Synthesis by Aerobic Oxidation of Primary Amines and in situ Generated Imines from Aldehydes and Ammonium Salt with Grubbs Catalyst
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Herein, a Grubbs-catalyzed route for the synthesis of nitriles via the aerobic oxidation of primary amines is reported. This reaction accommodates a variety of substrates, including simple primary amines, sterically hindered β,β-disubstituted amines, allylamine, benzylamines, and α-amino esters. Reaction compatibility with various functionalities is also noted, particularly with alkenes, alkynes, halogens, esters, silyl ethers, and free hydroxyl groups. The nitriles were also synthesized via the oxidation of imines generated from aldehydes and NH4OAc in situ. (Figure presented.).
- Utsumi, Tatsuki,Noda, Kenta,Kawauchi, Daichi,Ueda, Hirofumi,Tokuyama, Hidetoshi
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p. 3583 - 3588
(2020/08/05)
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- Copper-catalyzed Z-selective semihydrogenation of alkynes with hydrosilane: A convenient approach to cis-alkenes
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A copper catalyst generated in situ from widely available copper salt and imidazolium salt in the presence of t-BuOK showed high efficiency for the semihydrogenation of a wide range of internal and terminal alkynes to their corresponding alkenes without obvious over-reduction. Functional groups, such as hydroxyl, nitro, halides, and amino, etc. were tolerated. The Z/E ratios of the obtained alkenes were generally >99%. Finally, semireduction of bulky alkynes also went smoothly.
- Wang, Guang-Hui,Bin, Huai-Yu,Sun, Miao,Chen, Shu-Wei,Liu, Ji-Hong,Zhong, Chong-Min
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supporting information
p. 2175 - 2179
(2014/03/21)
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- AMINE COMPOUND AND PHARMACEUTICAL USE THEREOF
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Provided is a novel amine compound represented by the following formula (I) having a superior peripheral blood lymphocyte decreasing action and superior in the immunosuppressive action, rejection suppressive action and the like, which shows decreased side effects of, for example, bradycardia and the like, or a pharmaceutically acceptable acid addition salt thereof, or a hydrate thereof, or a solvate thereof. wherein each symbol is as defined in the specification.
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Page/Page column 150
(2010/04/25)
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- Novel Urokinase Inhibitors
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The present invention relates to novel compounds with inhibitory activity towards urokinase plasminogen activator (uPA); to methods for preparation of said uPA inhibitor compounds; to pharmaceutical compositions comprising said uPA inhibitor compounds; to
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Page/Page column 31
(2009/01/24)
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- Small, potent, and selective diaryl phosphonate inhibitors for urokinase-type plasminogen activator with in vivo antimetastatic properties
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A set of small nonpeptidic diaryl phosphonate inhibitors was prepared. Some of these inhibitors show potent and highly selective irreversible uPA inhibition. The biochemical and modeling data prove that the combination of a benzylguanidine moiety with a d
- Joossens, Jurgen,Ali, Omar M.,El-Sayed, Ibrahim,Surpateanu, Georgiana,Der Van Veken, Pieter,Lambeir, Anne-Marie,Setyono-Han, Buddy,Foekens, John A.,Schneider, Anneliese,Schmalix, Wolfgang,Haemers, Achtel,Augustyns, Koen
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p. 6638 - 6646
(2008/09/17)
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- NOVEL UROKINASE INHIBITORS
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The present invention relates to novel compounds with inhibitory activity towards urokinase plasminogen activator (uPA); to methods for preparation of said uPA inhibitor compounds; to pharmaceutical compositions comprising said uPA inhibitor compounds; to
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Page/Page column 68-70; 75-76
(2010/11/27)
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- NOVEL OXABISPIDINE COMPOUNDS AND THEIR USE IN THE TREATMENT OF CARDIAC ARRHYTHMIAS
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There is provided compounds of formula I, wherein R1, R2, R4, R41 to R46, A, B and G have meanings given in the description, which are useful in the prophylaxis and in the treatment of arrhythmias, in particular atrial and ventricular arrhythmias.
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Page/Page column 53
(2008/06/13)
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- PHENETANOLAMINE DERIVATIVES
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Compounds of formula (I) and salts, solvates, and physiologically functional derivatives thereof, useful for the prophylaxis or treatment of a clinical condition for which a selective β2-adrenoreceptor agonist is indicated, for example asthma or chronic o
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Page/Page column 51
(2010/02/11)
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- 2-QUINOXALINONE DERIVATIVES AS BRADYKININ ANTAGONISTS AND NOVEL COMPOUNDS
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2-Quinoxalinone derivatives are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway.
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Page/Page column 14
(2010/02/10)
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- NOVEL QUINOXALINONE DERIVATIVES AS BRADYKININ B1 ANTAGONISTS
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2-Quinoxalinone derivatives are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway.
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Page/Page column 24
(2010/02/07)
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- KETOPIPERAZINE DERIVATIVES AS BRADYKININ ANTAGONISTS
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Ketopiperazine derivatives are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway.
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- A new series of estrogen receptor modulators that display selectivity for estrogen receptor β
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A series of 1,3,5-triazine-based estrogen receptor (ER) modulators that are modestly selective for the ERβ subtype are reported. Compound 1, which displayed modest potency and selectivity for ERβ vs ERα, was identified via high-throughput screening utiliz
- Henke, Brad R.,Consler, Thomas G.,Go, Ning,Hale, Ron L.,Hohman, Dana R.,Jones, Stacey A.,Lu, Amy T.,Moore, Linda B.,Moore, John T.,Orband-Miller, Lisa A.,Robinett, R. Graham,Shearin, Jean,Spearing, Paul K.,Stewart, Eugene L.,Turnbull, Philip S.,Weaver, Susan L.,Williams, Shawn P.,Wisely, G. Bruce,Lambert, Millard H.
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p. 5492 - 5505
(2007/10/03)
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- 7-Substituted 5-amino-2-(2-furyl)pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as A2A adenosine receptor antagonists: A study on the importance of modifications at the side chain on the activity and solubility
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It was demonstrated in the early 1990s that adenosine exerts many physiological functions through the interaction with four different receptors, named A1, A2A, A2B, and A3. In the past few years, our group has been involved in the development of A2A antagonists, which led to the synthesis of SCH 58261 (1), the first potent and selective adenosine A2A antagonist, which has been widely used as a reference compound. In this paper, we present an extended series of pyrazolotriazolopyrimidines synthesized with the aim to investigate the influence of the substitutions on the pyrazole ring. The choice of the substituents was based on their capability to improve water solubility while retaining high affinity and selectivity at the human A2A adenosine receptor subtype. In this series, some structural characteristics that are important for activity, i.e., tricyclic structure, free amino group at 5-position, furan ring, and substituent at 7-position on the pyrazole moiety, have been maintained. We focused our attention on the nature of the phenyl ring substituent to improve water solubility. Following this strategy, we developed new compounds with good affinity and selectivity for A2A adenosine receptors, such as 8d (Ki 0.12 nM; hA1/hA2A ratio = 1025; Rm = 2.8), 8h (Ki 0.22; hA1/hA2A ratio = 9818; Rm = 3.4), 8i (Ki 0.18 nM; hA1/hA2A ratio = 994; Rm = 2.8), 8k (Ki 0.13 nM; hA1/hA2A ratio = 4430; Rm = 3.6), and 14b (Ki 0.19 nM; hA1/hA2A ratio = 2273; Rm = 2.7). All the new synthesized compounds have no significant interaction with either A2B or A3 receptor subtypes. This new series of compounds deeply enlightens some structural requirements to display high affinity and selectivity for the A2A adenosine receptor subtype, although our goal of identifying new compounds with increased water solubility was not completely achieved. On this basis, other strategies will be devised to improve this class of compounds with a profile that appears to be promising for treatment of neurodegenerative disorders, such as Parkinson's disease.
- Baraldi,Cacciari,Romagnoli,Spalluto,Monopoli,Ongini,Varani,Borea
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p. 115 - 126
(2007/10/03)
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- NAPHTHALENE AMIDES HAVING LEUKOTRIENE-ANTAGONISTIC ACTION
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Naphthalene amides of formula (I) wherein the substituent containing A is bound to the 6- or 7- position of the 2-naphthol system; the substituent containing B is bound to the benzene ring at any free position; R is hydrogen or methyl; R is hydrogen, fluorine, chlorine or -OCH3, which is bound to the naphthalene system at any positions except the 2- and the one occupied by the other substituent; R is hydrogen, fluorine, chlorine or bromine; A- is -CO-NR- or -NR-CO- group, wherein R is hydrogen or methyl; B is a 5-tetrazolyl or -COOR group, wherein R is hydrogen, a (C1-C4)-alkyl or a phenylalkyl group of less than 10 carbon atoms; m is 0 or 1; n and p are integers from 0 to 6, with the proviso that n + p is less or equal to 6; as well as the solvates and pharmaceutically acceptable salts thereof, have leukotriene antagonistic action.
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- Saturated heterocyclic carboxamide derivatives
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A saturated heterocyclic carboxamide derivative of the following general formula (I) and salts thereof which have platelet activating factor (PAF) antagonizing activity. STR1
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- Benzamidine derivatives
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The present invention relates to benzamidine derivatives corresponding to the general formula STR1 in which: A represents a linear or branched alkyl chain containing from 3 to 9 carbon atoms; and X represents the oxygen atom or a direct bond, with the restriction that if X represents a direct bond, the benzamidine and the alkanol group are located in the para position, and also the pharmaceutically acceptable salts of the products of the formula (I); it also relates to a process for the preparation of the products of the formula (I) and the drugs for external use which contain a product of the formula (I).
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- Process for preparing urokinase complex
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This invention provides a process for preparing a fibrin-adsorable protein-urokinase complex characterized by reacting a protein adsorbable by fibrin with urokinase in the presence of a protein coupling reagent represented by the formula STR1 wherein R is phenylene or cycloalkylene, A is lower alkylene, B is lower alkylene which may optionally be substituted by lower alkylthio or phenyl-lower alkylthio, and l, m and n are each 0 or 1 provided that l, m and n are not 0 at the same time. The complex is useful as a thrombolytic agent.
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