62501-70-6Relevant academic research and scientific papers
Enantioselective Access to Chiral 2-Substituted 2,3-Dihydrobenzo[1,4]dioxane Derivatives through Rh-Catalyzed Asymmetric Hydrogenation
Yin, Xuguang,Huang, Yi,Chen, Ziyi,Hu, Yang,Tao, Lin,Zhao, Qingyang,Dong, Xiu-Qin,Zhang, Xumu
, p. 4173 - 4177 (2018/07/29)
Rh-catalyzed asymmetric hydrogenation of various benzo[b][1,4]dioxine derivatives was successfully developed to prepare chiral 2-substituted 2,3-dihydrobenzo[1,4]dioxane derivatives using ZhaoPhos and N-methylation of ZhaoPhos ligands with high yields and excellent enantioselectivities (up to 99% yield, >99% enantiomeric excess (ee), turnover number (TON) = 24 000). Moreover, this asymmetric hydrogenation methodology, as the key step with up to 10 000 TON, was successfully applied to develop highly efficient synthetic routes for the construction of some important biologically active molecules, such as MKC-242, WB4101, BSF-190555, and (R)-doxazosin·HCl.
DOPAMINE D2 RECEPTOR LIGANDS
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Page/Page column 150, (2016/07/05)
The present invention relates to novel dopamine D2 receptor ligands. The invention further relates to functionally-biased dopamine D2 receptor ligands and the use of these compounds for treating or preventing central nervous system and systemic disorders associated with dysregulation of dopaminergic activity. The present invention relates to novel compounds that modulate dopamine D2 receptors. In particular, compounds of the present invention show functional selectivity at the dopamine D2 receptors and exhibit selectivity downstream of the D2 receptors, on the 0- arrestin pathway and/or on the cAMP pathway.
Pd-catalyzed asymmetric intramolecular aryl c-o bond formation with SDP(O) ligand: Enantioselective synthesis of (2,3-Dihydrobenzo[ b ][1,4]dioxin-2-yl)methanols
Shi, Jialing,Huang, Yusha,Cai, Qian,Wang, Ting,Zhang, Xinhao,Wu, Yun-Dong
supporting information, p. 840 - 843 (2015/04/14)
Employing a chiral spirodiphosphine monoxide ligand with 1,1′-spirobiindane backbone (SDP(O)), a desymmetrization strategy of Pd-catalyzed intramolecular asymmetric aryl C-O coupling of 2-(2-halophenoxy)propane-1,3-diols, was developed. The SDP(O) ligand shows much better results than its SDP counterpart. The protocol provides an efficient and highly enantioselective method for the synthesis of 2-hydroxymethyl-1,4-benzodioxanes. Density functional theory studies provide a model that accounts for the origin of the enantioselectivity.
Orally active ghrelin receptor inverse agonists and their actions on a rat obesity model
Takahashi, Bitoku,Funami, Hideaki,Iwaki, Takehiko,Maruoka, Hiroshi,Shibata, Makoto,Koyama, Makoto,Nagahira, Asako,Kamiide, Yoshiyuki,Kanki, Satomi,Igawa, Yoshiyuki,Muto, Tsuyoshi
, p. 4792 - 4803 (2015/08/03)
A series of 2-alkylamino nicotinamide analogs was prepared as orally active ghrelin receptor (ghrelinR) inverse agonists. Starting from compound 1, oral bioavailability was improved by modifying metabolically unstable sites and reducing molecular weight. Brain-permeable compound 33 and compound 24 with low brain permeability were tested in rat models of obesity; 30 mg/kg of compound 33 suppressed weight gain. PK/PD analysis revealed that the anti-obesity effect of ghrelinR inverse agonists depends on their brain concentrations.
Novel, broad-spectrum anticonvulsants containing a sulfamide group: Pharmacological properties of (S)- N -[(6-chloro-2,3-dihydrobenzo[1,4]dioxin-2- yl)methyl]sulfamide (JNJ-26489112)
McComsey, David F.,Smith-Swintosky, Virginia L.,Parker, Michael H.,Brenneman, Douglas E.,Malatynska, Ewa,White, H. Steve,Klein, Brian D.,Wilcox, Karen S.,Milewski, Michael E.,Herb, Mark,Finley, Michael F. A.,Liu, Yi,Lubin, Mary Lou,Qin, Ning,Reitz, Allen B.,Maryanoff, Bruce E.
, p. 9019 - 9030 (2014/01/06)
Broad-spectrum anticonvulsants are of considerable interest as antiepileptic drugs, especially because of their potential for treating refractory patients. Such "neurostabilizers" have also been used to treat other neurological disorders, including migraine, bipolar disorder, and neuropathic pain. We synthesized a series of sulfamide derivatives (4-9, 10a-i, 11a, 11b, 12) and evaluated their anticonvulsant activity. Thus, we identified promising sulfamide 4 (JNJ-26489112) and explored its pharmacological properties. Compound 4 exhibited excellent anticonvulsant activity in rodents against audiogenic, electrically induced, and chemically induced seizures. Mechanistically, 4 inhibited voltage-gated Na+ channels and N-type Ca2+ channels and was effective as a K+ channel opener. The anticonvulsant profile of 4 suggests that it may be useful for treating multiple forms of epilepsy (generalized tonic-clonic, complex partial, absence seizures), including refractory (or pharmacoresistant) epilepsy, at dose levels that confer a good safety margin. On the basis of its pharmacology and other favorable characteristics, 4 was advanced into human clinical studies.
2,3-DIHYDROBENZO[l,4] DIOXIN-2-YLMETHYL DERIVATIVES AS ALPHA2C ANTAGONISTS FOR USE IN THE TREATMENT OF PERIPHERIC AND CENTRAL NERVOUS SYSTEME DISEASES
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Page/Page column 89, (2009/03/07)
Compounds of formula (I), wherein X, Z, R1-R4, and m are as defined in the claims, exhibit alpha2C antagonistic activity and are thus useful for the treatment of diseases and conditions of the peripheric system and the central nervous system (CNS).
USE OF BENZO-FUSED HETEROCYCLE SULFAMIDE DERIVATIVES AS NEUROPROTECTIVE AGENTS
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Page/Page column 13, (2010/11/27)
The present invention is a methods for neuroprotection, for treating an acute neurodegenerative disorder, for treating a chronic neurodegenerative disorder and/or for preventing neuron death or damage following brain, head and/or spinal cord trauma or inj
USE OF BENZO-FUSED HETEROCYCLE SULFAMIDE DERIVATIVES FOR THE TREATMENT OF SUBSTANCE ABUSE AND ADDICTION
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Page/Page column 13, (2010/11/27)
The present invention is a method for the treatment of alcohol abuse and/or addiction comprising administering to a subject in need thereof a therapeutically effective amount of one or more novel benzo-fused heterocycle sulfamide derivatives of formula (I
USE OF BENZO-FUSED HETEROCYLE SULFAMIDE DERIVATIVES FOR THE TREATMENT OF MANIA AND BIPOLAR DISORDER
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Page/Page column 15-16, (2010/11/27)
The present invention is a method for the treatment of mania and/or bipolar disorder comprising administering to a subject in need thereof a therapeutically effective amount of one or more novel benzo-fused heterocycle sulfamide derivatives of formula (I)
USE OF BENZO-FUSED HETEROCYCLE SULFAMIDE DERIVATIVES FOR THE TREATMENT OF OBESITY
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Page/Page column 34, (2010/11/27)
The present invention is a method for the treatment of obesity, for promoting weight loss and / or suppressing appetite comprising administering to a subject in need thereof a therapeutically effective amount of one or more novel benzo-fused heterocycle s
