70807-22-6Relevant academic research and scientific papers
Unconventional Rose Odorants: Serendipitous Discovery and Unique Olfactory Properties of 2,2-Bis(prenyl)-3-oxobutyronitrile and Its Derivatives
Hauser, Nicole,Kraft, Philip,Carreira, Erick M.
, p. 4490 - 4500 (2018)
2,2-Bis(3-methylbut-2-enyl)-3-oxobutanenitrile [2,2-bis(prenyl)-3-oxobutyronitrile], an unusual bifunctional nitrile odorant with a fruity rosy, green odor was found to exhibit surprising differences in its detection thresholds (0.25 ng/L air for hyperosm
NEW ANTHELMINTIC COMPOUNDS
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Page/Page column 88; 107-108, (2020/05/28)
The present invention relates to novel compounds of general formula (I) with A being A1 or A2, and in which T, X, Y, Ro, R1, R10 and R11 are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for the treatment, control and/or prevention of diseases, in particular of helminth infections, as a sole agent or in combination with other active ingredients.
Phenyl substituted fused tricyclic compound and uses thereof
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Paragraph 0182; 00187; 0188, (2019/05/16)
The present invention relates to a phenyl substituted fused tricyclic compound and uses thereof, further to a pharmaceutical composition containing the compound. According to the present invention, the compound or the pharmaceutical composition can be use
Potent and Selective Human Neutrophil Elastase Inhibitors with Novel Equatorial Ring Topology: In vivo Efficacy of the Polar Pyrimidopyridazine BAY-8040 in a Pulmonary Arterial Hypertension Rat Model
Von Nussbaum, Franz,Li, Volkhart M.,Meibom, Daniel,Anlauf, Sonja,Bechem, Martin,Delbeck, Martina,Gerisch, Michael,Harrenga, Axel,Karthaus, Dagmar,Lang, Dieter,Lustig, Klemens,Mittendorf, Joachim,Sch?fer, Martina,Sch?fer, Stefan,Schamberger, Jens
supporting information, p. 199 - 206 (2016/01/30)
Human neutrophil elastase (HNE) is a key driver of inflammation in many cardiopulmonary and systemic inflammatory and autoimmune conditions. Overshooting high HNE activity is the consequence of a disrupted protease-antiprotease balance. Accordingly, there has been an intensive search for potent and selective HNE inhibitors with suitable pharmacokinetics that would allowing oral administration in patients. Based on the chemical probe BAY-678 and the clinical candidate BAY 85-8501 we explored further ring topologies along the equator of the parent pyrimidinone lead series. Novel ring systems were annulated in the east, yielding imidazolo-, triazolo-, and tetrazolopyrimidines in order to ensure additional inhibitor-HNE contacts beyond the S1 and the S2 pocket of HNE. The western annulation of pyridazines led to the polar pyrimidopyridazine BAY-8040, which combines excellent potency and selectivity with a promising pharmacokinetic profile. In vivo efficacy with regard to decreasing cardiac remodeling and amelioration of cardiac function was shown in a monocrotaline-induced rat model for pulmonary arterial hypertension. This demonstrated in vivo proof of concept in animals. Exploring new rings! Human neutrophil elastase (HNE) is a driver of inflammation in pulmonary arterial hypertension (PAH). Herein we describe the discovery of BAY-8040, a small-molecule inhibitor with nanomolar potency and good pharmacokinetics. BAY-8040 shows in vivo efficacy in a PAH rat model, thereby demonstrating proof of concept in animals.
PYRAZOLOPYRIMIDINE DERIVATIVES AS PI3 KINASE INHIBITORS
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Page/Page column 68; 69, (2013/03/26)
The present invention relates to compounds of formula (I) in which R1, R2, R3 and n have the meaning given in the specification and also relates to the use of these pyrazolopyrimidine derivatives for the modulation, notably the inhibition of the activity or function of the phosphoinositide 3'OΗ kinase family (hereinafter PI3 kinases), wherein the compounds of formula (I) are described as selective inhibitors of PI3K[beta] activity.
N-heterocyclic carbene-catalyzed annulation of α-cyano-1,4-diketones with ynals
Romanov-Michailidis, Fedor,Besnard, Celine,Alexakis, Alexandre
supporting information, p. 4906 - 4909,4 (2012/12/12)
In this paper, the first stereoselective annulation reaction between r-cyano-1,4-diketones and ynals, mediated by catalytic amounts of a triazolium salt precatalyst and cocatalytic amounts of a weak carboxylate base, is disclosed. The title transformation proceeds smoothly under mild reaction conditions and generates three contiguous stereogenic centers, one of which is a quaternary acetal carbon. This reaction tolerates a wide variety of electronically distinct substituents on both reaction partners and affords privileged bicyclic scaffolds in 61-90% isolated yields and with up to 20:1 diastereomeric preference.
N-heterocyclic carbene-catalyzed annulation of α-cyano-1,4-diketones with ynals
Romanov-Michailidis, Fedor,Besnard, Céline,Alexakis, Alexandre
supporting information, p. 4906 - 4909 (2013/01/15)
In this paper, the first stereoselective annulation reaction between r-cyano-1,4-diketones and ynals, mediated by catalytic amounts of a triazolium salt precatalyst and cocatalytic amounts of a weak carboxylate base, is disclosed. The title transformation proceeds smoothly under mild reaction conditions and generates three contiguous stereogenic centers, one of which is a quaternary acetal carbon. This reaction tolerates a wide variety of electronically distinct substituents on both reaction partners and affords privileged bicyclic scaffolds in 61-90% isolated yields and with up to 20:1 diastereomeric preference.
5-ARYL-SUBSTITUTED DIHYDROPYRIDOPYRIMIDINES AND DIHYDROPYRIDAZINES AND USE THEREOF AS MINERAL CORTICOID ANTAGONISTS
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Page/Page column 18, (2010/03/02)
The present application relates to novel aryl-substituted heterobicyclic compounds, a process for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for the manufacture of medicaments for the treatment and/or prop
SUBSTITUTED 4-ARYL-1,4-DIHYDRO-1,6-NAPHTHYRIDINES AND USE THEREOF
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Page/Page column 17, (2010/12/29)
The present application relates to novel substituted 4-aryl-1,4-dihydro-1,6-naphthyridines, a process for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, especially cardiovascular disorders.
Design and synthesis of 3-(2-pyridyl)pyrazolo[1,5-a]pyrimidines as potent CRF1 receptor antagonists
Huang, Charles Q.,Wilcoxen, Keith M.,Grigoriadis, Dimitri E.,McCarthy, James R.,Chen, Chen
, p. 3943 - 3947 (2007/10/03)
A series of 3-(2-pyridyl)pyrazolo[1,5-a]pyrimidines was designed and synthesized as antagonists for the corticotrophin-releasing factor-1 (CRF 1) receptor. Several compounds such as 20c (Ki=10nM) exhibited good binding affinities at the CRF1 receptor. In addition, 20c had adequate solubility in water.
