- ORGANIC ELECTROLUMINESCENT DEVICE AND ORGANOMETALLIC COMPOUND FOR THE SAME
-
The present application relates to an organometallic compound represented by Formula 1 and an organic electroluminescent device, in which the organic electroluminescent device comprises the organometallic compound represented by Formula 1 in an emission l
- -
-
Paragraph 0252-0254; 0259-0260
(2021/05/15)
-
- One-pot synthesis of 1-monosubstituted-1, 2, 3-triazoles from 2-methyl-3-butyn-2-ol
-
An efficient method for the synthesis of 1-monosubstituted-1, 2, 3-triazoles from 2-methyl-3-butyn-2-ol under copper catalyst conditions has been developed through a one-step one-pot sequence. This method provides a concise and efficient pathway to synthesize 1-monosubstituted-1, 2, 3-triazole derivatives in good to excellent yields.
- Liu, Yaowen,Han, Chunmei,Ma, Xinyuan,Yang, Jianhua,Feng, Xuepu,Jiang, Yubo
-
supporting information
p. 650 - 653
(2018/01/15)
-
- One-Pot Synthesis of 1-Monosubstituted 1,2,3-Triazoles from Propargyl Alcohol
-
A one-pot synthesis of 1-monosubstituted-1,2,3-triazoles from propargyl alcohol and various aryl azides was achieved. This simple method provides concise and efficient access to various 1-monosubstituted 1,2,3-triazole derivatives through a three-step one
- Han, Chunmei,Dong, Suping,Zhang, Wensheng,Chen, Zhen
-
supporting information
p. 673 - 677
(2018/03/10)
-
- Discovery of (S)-3-(3-(3,5-Dimethyl-1 H-pyrazol-1-yl)phenyl)-4-((R)-3-(2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl)pyrrolidin-1-yl)butanoic Acid, a Nonpeptidic αvβ6 Integrin Inhibitor for the Inhaled Treatment of Idiopathic Pulmonary Fibrosis
-
A series of 3-aryl(pyrrolidin-1-yl)butanoic acids were synthesized using a diastereoselective route, via a rhodium catalyzed asymmetric 1,4-addition of arylboronic acids in the presence of (R)-BINAP to a crotonate ester to provide the (S) absolute configuration for the major product. A variety of aryl substituents including morpholine, pyrazole, triazole, imidazole, and cyclic ether were screened in cell adhesion assays for affinity against αvβ1, αvβ3, αvβ5, αvβ6, and αvβ8 integrins. Numerous analogs with high affinity and selectivity for the αvβ6 integrin were identified. The analog (S)-3-(3-(3,5-dimethyl-1H-pyrazol-1-yl)phenyl)-4-((R)-3-(2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl)pyrrolidin-1-yl)butanoic acid hydrochloride salt was found to have very high affinity for αvβ6 integrin in a radioligand binding assay (pKi = 11), a long dissociation half-life (7 h), very high solubility in saline at pH 7 (>71 mg/mL), and pharmacokinetic properties commensurate with inhaled dosing by nebulization. It was selected for further clinical investigation as a potential therapeutic agent for the treatment of idiopathic pulmonary fibrosis.
- Procopiou, Panayiotis A.,Anderson, Niall A.,Barrett, John,Barrett, Tim N.,Crawford, Matthew H. J.,Fallon, Brendan J.,Hancock, Ashley P.,Le, Joelle,Lemma, Seble,Marshall, Richard P.,Morrell, Josie,Pritchard, John M.,Rowedder, James E.,Saklatvala, Paula,Slack, Robert J.,Sollis, Steven L.,Suckling, Colin J.,Thorp, Lee R.,Vitulli, Giovanni,Macdonald, Simon J. F.
-
supporting information
p. 8417 - 8443
(2018/09/25)
-
- NAPHTHYRIDINE DERIVATIVES AS ALPHA V BETA 6 INTEGRIN ANTAGONISTS FOR THE TREATMENT OF E.G. FIBROTIC DISEASES
-
A compound of formula (I) or a salt thereof wherein R1 represents a five-membered aromatic heterocycle selected from a N- or a C-linked mono- or di-substituted pyrazole, an N- or a C-linked optionally mono- or di-substituted triazole or an N- or a C-linked optionally mono-or di-substituted imidazole, which five-membered aromatic heterocycle may be substituted by one or two of the groups selected from a hydrogen atom, a methyl group, an ethyl group, a fluorine atom, a hydroxymethyl group, a 2-hydroxypropan-2-yl group, a trifluoromethyl group, a difluoromethyl group or a fluoromethyl group, except that when R1 represents an N-linked mono-or di-substituted pyrazole, R1 does not represent 3,5-Dimethyl-1H- pyrazol-1-yl, 5-Methyl-1H-pyrazol-1-yl, 5-Ethyl-3-methyl-1H-pyrazol-1-yl, 3,5-Diethyl-1H-pyrazol-1- yl, 4-Fluoro-3,5-dimethyl-1H-pyrazol-1-yl, 3-Methyl-1H- pyrazol-1-yl or 1H- pyrazol-1-yl.
- -
-
Page/Page column 38
(2016/04/20)
-
- N-PIPERIDIN-4-YL DERIVATIVES
-
The invention relates to a N-piperidin-4-yl derivative having the general Formula I or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same and to the use of said N-piperidin-4-yl derivatives for the treatment and prevention of endometriosis, for the treatment and prevention of pre-menopausal and peri-menopausal hormone-dependent breast cancer, for contraception, or for the treatment of uterine fibroids or other menstrual-related disorders.
- -
-
Page/Page column 41
(2013/04/10)
-
- Facile and quick synthesis of 1-monosubstituted aryl 1,2,3-triazoles: A copper-free [3+2] cycloaddition
-
An efficient copper-free synthesis of 1-monosubstituted aryl 1,2,3-triazoles from sodium acetylide and aryl azides was developed, which was found suitable for various aryl azides and completed within 15 min at room temperature with moderate to excellent y
- Jiang, Yubo,Kuang, Chunxiang,Yang, Qing
-
experimental part
p. 289 - 292
(2011/02/28)
-
- A convenient synthesis of 1-substituted 1,2,3-triazoles via CuI/Et 3N catalyzed 'click chemistry' from azides and acetylene gas
-
Copper(I)-catalyzed 'click chemistry' using acetylene gas was successfully explored under mild conditions. 1-Substituted-1,2,3-triazoles were conveniently synthesized from the corresponding aromatic and aliphatic azides. Georg Thieme Verlag Stuttgart.
- Wu, Lu-Yong,Xie, Yong-Xin,Chen, Zi-Sheng,Niu, Yan-Ning,Liang, Yong-Min
-
experimental part
p. 1453 - 1456
(2009/10/23)
-