- Bipolar fluorescent material based on benzoquinary heterocyclic ring and preparation method thereof and organic electroluminescent device
-
The present invention discloses a bipolar fluorescent material based on a benzoquinary heterocyclic ring and a preparation method thereof with an organic electroluminescent device, the bipolar fluorescent material having the following structure shown: or
- -
-
Paragraph 0071-0075; 0087-0091
(2022/01/08)
-
- Five-membered heterocyclic oxo carboxylic acid compound and medical application thereof
-
The invention relates to a five-membered heterocyclic oxo carboxylic acid compound and a medical application thereof. Specifically, the invention relates to a compound, a pharmaceutical salt, a prodrug, a hydrate, a solvate or a crystal form as shown in a formula (I), and also relates to a preparation method of the compound, a pharmaceutical composition containing the compound and an application of the pharmaceutical composition as a secretion regulator of interferon type I, especially as an STING agonist in preparation of medicines for preventing and/or treating I-type interferon related diseases.
- -
-
Paragraph 0707; 0712-0714
(2021/05/01)
-
- Rhodium-Catalyzed Intermolecular Cyclopropanation of Benzofurans, Indoles, and Alkenes via Cyclopropene Ring Opening
-
The generation of metal carbenoids via ring opening of cyclopropenes by transition metals offers a simple entry into highly reactive intermediates. Herein, we describe a diastereoselective intermolecular rhodium-catalyzed cyclopropanation of heterocycles and alkenes using cyclopropenes as carbene precursors with a low loading of a commercially available rhodium catalyst. The reported method is scalable and could be performed with catalyst loadings as low as 0.2 mol %, with no impact to the reaction yield or selectivity.
- Jeyaseelan, Rubaishan,Lautens, Mark,Ross, Rachel J.
-
-
- Biocatalytic Strategy for Highly Diastereo- and Enantioselective Synthesis of 2,3-Dihydrobenzofuran-Based Tricyclic Scaffolds
-
2,3-Dihydrobenzofurans are key pharmacophores in many natural and synthetic bioactive molecules. A biocatalytic strategy is reported here for the highly diastereo- and enantioselective construction of stereochemically rich 2,3-dihydrobenzofurans in high enantiopurity (>99.9% de and ee), high yields, and on a preparative scale via benzofuran cyclopropanation with engineered myoglobins. Computational and structure-reactivity studies provide insights into the mechanism of this reaction, enabling the elaboration of a stereochemical model that can rationalize the high stereoselectivity of the biocatalyst. This information was leveraged to implement a highly stereoselective route to a drug molecule and a tricyclic scaffold featuring five stereogenic centers via a single-enzyme transformation. This work expands the biocatalytic toolbox for asymmetric C–C bond transformations and should prove useful for further development of metalloprotein catalysts for abiotic carbene transfer reactions.
- Vargas, David A.,Khade, Rahul L.,Zhang, Yong,Fasan, Rudi
-
p. 10148 - 10152
(2019/07/04)
-
- 1,3-disubstituted ketene compound and application thereof
-
The invention relates to a 1,3-disubstituted ketene compound with a structure as shown in a formula (I) and application thereof. The compound mainly activates a PPAR (Peroxisome Proliferators-Activated Receptor) alpha, and also has excitation activity for PPPA delta and PPPA gamma. The 1,3-disubstituted ketene compound can be used for treating various diseases related to the PPAR regulation abnormality, such as NASH (nonalcoholic steatohepatitis), and particularly treating nonalcoholic hepatitis, also has potentials for treating diabetes, obesity, fibrotic diseases, cardiovascular diseases (comprising a heart failure, atherosclerosis and the like), kidney diseases (comprising chronic nephrosis, a kidney failure and the like), brain degenerative diseases (comprising the alzheimer disease and the like) and the like, and has higher application value. The formula is shown in the description.
- -
-
-
- Visible light-induced monofluoromethylenation of heteroarenes with ethyl bromofluoroacetate
-
Visible light-induced monofluoromethylenation of benzofurans and benzothiophenes with ethyl bromofluoroacetate was developed. This method provided a convenient access to novel α-fluoro-α-heteroarylesters under mild reaction conditions.
- Yu, Wei,Xu, Xiu-Hua,Qing, Feng-Ling
-
p. 6564 - 6567
(2016/08/09)
-
- 7-process for the preparation of bromide and furan
-
The invention belongs to the field of organic synthesis, and particularly relates to a preparation method of 7-bromobenzofuran. The preparation method comprises the following steps: reacting ortho-bromophenol and 2-bromo-1,1-dimethoxyethane or 2-chloro-1,
- -
-
-
- SPIRO-OXADIAZOLINE COMPOUNDS AS AGONISTS OF α-7-NICOTINIC ACETYLCHOLINE RECEPTORS
-
The present invention relates to novel spiro-oxadiazoline compounds that are suitable as agonists or partial agonists of a7-nAChR, and pharmaceutical compositions of the same, methods of preparing these compounds and compositions, and the use of these compounds and compositions in methods of maintaining, treating and/or improving cognitive function. In particular, methods of administering a spiro-oxadiazoline cx7-nAChR agonist or partial agonist, to a patient in need thereof, for example a patient with a cognitive deficiency and/or a desire to enhance cognitive function, that may derive a benefit therefrom.
- -
-
-
- NOVEL TRICYCLIC CALCIUM SENSING RECEPTOR ANTAGONISTS
-
Novel tricyclic compounds of Formula (I) and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing osteoporosis and similar conditions. The compounds are effective as calcium sensing receptor antagonists. Pharmaceutical compositions and methods of treatment are also included.
- -
-
-
- NOVEL TRICYCLIC CALCIUM SENSING RECEPTOR ANTAGONISTS FOR THE TREATMENT OF OSTEOPOROSIS
-
Novel tricyclic compounds of the formula (I): and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing osteoporosis and similar conditions. The compounds are effective as calcium sensing receptor antagonists. Pharmaceutical compositions and methods of treatment are also included.
- -
-
-
- Discovery of novel tricyclic indole derived inhibitors of HCV NS5B RNA dependent RNA polymerase
-
The characterization of HCV genome has identified various vital functional proteins involved in the life cycle of hepatitis C virus. This has resulted in many novel enzymatic targets that are potential for development of therapeutic agents. The HCV RNA de
- Venkatraman, Srikanth,Velazquez, Francisco,Gavalas, Stephen,Wu, Wanli,Chen, Kevin X.,Nair, Anilkumar G.,Bennett, Frank,Huang, Yuhua,Pinto, Patrick,Jiang, Yueheng,Selyutin, Oleg,Vibulbhan, Bancha,Zeng, Qingbei,Lesburg, Charles,Duca, Jose,Huang, Hsueh-Cheng,Agrawal, Sony,Jiang, Chuan-Kui,Ferrari, Eric,Li, Cheng,Kozlowski, Joseph,Rosenblum, Stuart,Shih, Neng-Yang,Njoroge, F. George
-
p. 2007 - 2017
(2013/04/24)
-
- Synthesis of piperazino-substituted benzo[b]furans as potential CNS agents
-
The synthesis of a series of substituted benzofurans is reported. Selected compounds have been shown to bind strongly and with high selectivity to the serotonin receptor 5-HT2A in the presence of the receptor 5-HT 7 in vitro.
- Klenc, Jeff,Strekowski, Lucjan
-
p. 249 - 252
(2011/06/10)
-
- CARBINOL DERIVATIVES HAVING HETEROCYCLIC LINKER
-
[Object] It is to provide a novel LXRβ agonist useful as a preventative and/or therapeutic agent for atherosclerosis; arteriosclerosis such as those resulting from diabetes; dyslipidemia; hypercholesterolemia; lipid-related diseases; inflammatory diseases that are caused by inflammatory cytokines; skin diseases such as allergic skin diseases; diabetes; or Alzheimer's disease. [Solving Means] A carbinol compound represented by the following general formula (I) or salt thereof, or their solvate: (wherein, each V and W independently show N or C—R7; each X and Y independently show CH2, C═O, SO2, etc; Z shows CH or N; each R1, R2 and R7 independently show a hydrogen atom, C1-8 alkyl group, etc.; R3 shows C1-8 alkyl group; R4 shows an optionally substituted C6-10 aryl group or an optionally substituted 5- to 11-membered heterocyclic group; R5 and R6 show a hydrogen atom, etc.; L shows a C1-8 alkyl chain optionally substituted with an oxo group, etc.; and n shows any integer of 0 to 2.)
- -
-
Page/Page column 42
(2010/12/29)
-
- NOVEL LACTAM COMPOUND
-
The present invention provides a novel lactam compound, a sugar transport enhancement agent containing this compound as an active ingredient, an agent for the prevention and/or treatment of diabetes mellitus, diabetic peripheral neuropathy, diabetic nephr
- -
-
Page/Page column 13
(2010/11/29)
-
- PIPERIDINE AND MORPHOLINE RENIN INHIBITORS
-
Described are compounds which are orally active and bind to renin to inhibit its activity. They are useful in the treatment or amelioration of diseases associated with renin activity. Also described are methods of use of these compounds for treating or ameliorating a renin mediated disorder in a subject.
- -
-
-
- Aminoalkylbenzofurans as serotonin (5-HT(2c)) agonists
-
The present invention provides serotonergic aminoalkylbenzofurans of Formula (I): where R, R1, R2, R3, R4, R4′, R5, R5′, and R12 are as described in the specification.
- -
-
Page/Page column 21
(2010/11/08)
-
- SEROTONERGIC BENZOFURANS
-
The present invention provides serotonergic benzofurans of Formula (I): where A, R, R, R, R, and R are as described in the specification.
- -
-
Page/Page column 16
(2010/02/04)
-
- BENZOFURYLPIPERAZINES AND BENZOFURYLHOMOPIPERAZINES: SEROTONIN AGONISTS
-
The present invention provides serotonergic benzofurylpiperazines of Formula I: where: A is a piperazine of formula: and R, R1, R2, R3, R4, R5, R5', R6, R6', R7, R7', R8, and R8' are as described in the specification.
- -
-
-
- Azepine derivatives having effects on serotonin related systems
-
The present invention provides compounds of formula I and a method of inhibiting the reuptake of serotonin, antagonizing the 5-HT1Areceptor and antagonizing the 5-HT2Areceptor which comprises administering to a subject in need of suc
- -
-
-
- Piperidine derivatives having effects on serotonin related systems
-
The present invention provides the compounds of the following formula: Wherein the variables are as defined in the specification and a method for inhibiting the reuptake of seretonin, antagonizing the 5-HT1Areceptor and antagonizing the 5-HT2Areceptor which comprises administering to a subject in need of such treatment an effective amount of the compound of above formula.
- -
-
-
- Pyrrolidine and pyrroline derivatives having effects on serotonin related systems
-
The present invention provides the compounds of the following formula (I): and a method for inhibiting the reuptake of seretonin, antagonizing the 5-HT1Areceptor and antagonizing the 5-HT2Areceptor which comprises administering to a subject in need of such treatment an effective amount of formula (I).
- -
-
Page column 38
(2010/02/05)
-
- Piperazine derivatives as therapeutic agents
-
Substituted piperazine compounds of formula I STR1 in which HET is a substituted pyrazole, imidazole or 1,2,4-triazole have utility in the treatment of central nervous system disorders, for example depression, anxiety, psychoses (for example schizophrenia), tardive dyskinesia, Parkinson's disease, obesity, hypertension, Tourette's syndrome, sexual dysfunction, drug addiction, drug abuse, cognitive disorders, Alzheimer's disease, senile dementia, obsessive-compulsive behaviour, panic attacks, social phobias, eating disorders and anorexia, cardiovascular and cerebrovascular disorders, non-insulin dependent diabetes mellitus, hyperglycaemia, constipation, arrhythmia, disorders of the neuroendocrine system, stress, prostatic hypertrophy, and spasticity.
- -
-
-
