cas 105655-01-4, 6-Bromo-3,4-dihydro-2H-benzo[1,4]oxazine hydrochloride

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Design, synthesis, and bioevaluation of substituted phenyl isoxazole analogues as herbicide safeners
Herbicide safeners enhance herbicide detoxification in crops without affecting target weed sensitivity. To enhance crop tolerance to the toxicity-related stress caused by the herbicide acetochlor (ACT), a new class of substituted phenyl isoxazole derivatives was designed by an intermediate derivatization method as herbicide safeners. Microwave-assisted synthesis was used to prepare the phenyl isoxazole analogues, and all of the structures were confirmed via IR, 1H NMR, 13C NMR, and HRMS. Compound I-1 was further characterized by X-ray diffraction analysis. Bioassay results showed that most of the obtained compounds provided varying degrees of safening against ACT-induced injury by increasing the corn growth recovery, glutathione content, and glutathione S-transferase activity. In particular, compound I-20 showed excellent safener activity against ACT toxicity, comparable to that of the commercial safener benoxacor. Gaussian calculations have been performed and the results indicated that the nucleophilic ability of compound I-20 is higher than that of benoxacor, thus the activity is higher than that of benoxacor. These findings demonstrate that phenyl isoxazole derivatives possess great potential for protective management in cornfields.
Fu, Ying,Gao, Shuang,Gao, Ying-Chao,Guo, Ke-Liang,Li, Juan-Juan,Wang, Zi-Wei,Ye, Fei,Zhao, Li-Xia
p. 10550 - 10559
(2020)
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Simple and efficient synthesis of novel N -dichloroacetyl-3,4-dihydro-2 H -1,4-benzoxazines
An easy synthetic route to N -dichloroacetyl- 3,4-dihydro-2 H -1,4-benzoxazine derivatives 3 involves cyclization of 2-aminophenols 1 with 1,2-dibromoethane and subsequent acylation of the resultant 3,4-dihydro- 2 H -1,4-benzoxazine derivatives 2 with dichloroacetyl chloride. All compounds were characterized by IR, 1 H NMR, 13 C NMR, ESI-MS and elemental analysis. The structure of 3a was determined by X-ray crystallographic analysis.
Fu, Ying,Qu, Li-Hua,Zhang, Shan-Shan,Ye, Fei,Zhao, Li-Xia,Gao, Shuang,Xing, Zhi-Yong
p. 143 - 146
(2012)
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Synthesis, docking, 3-D-qsar, and biological assays of novel indole derivatives targeting serotonin transporter, dopamine D2 receptor, and mao-a enzyme: In the pursuit for potential multitarget directed ligands
A series of 27 compounds of general structure 2,3-dihydro-benzo[1,4]oxazin-4-yl)-2-{4-[3-(1H-3indolyl)-propyl]-1-piperazinyl}-ethanamides, Series I: 7(a-o) and (2-{4-[3-(1H-3-indolyl) -propyl]-1-piperazinyl}-acetylamine)-N-(2-morfolin-4-yl-ethyl)-fluorinated benzamides Series II: 13(a-l) were synthesized and evaluated as novel multitarget ligands towards dopamine D2 receptor, serotonin transporter (SERT), and monoamine oxidase-A (MAO-A) directed to the management of major depressive disorder (MDD). All the assayed compounds showed affinity for SERT in the nanomolar range, with five of them displaying Ki values from 5 to 10 nM. Compounds 7k, Ki = 5.63 ± 0.82 nM, and 13c, Ki = 6.85 ± 0.19 nM, showed the highest potencies. The affinities for D2 ranged from micro to nanomolar, while MAO-A inhibition was more discrete. Nevertheless, compounds 7m and 7n showed affinities for the D2 receptor in the nanomolar range (7n: Ki = 307 ± 6 nM and 7m: Ki = 593 ± 62 nM). Compound 7n was the only derivative displaying comparable affinities for SERT and D2 receptor (D2/SERT ratio = 3.6) and could be considered as a multitarget lead for further optimization. In addition, docking studies aimed to rationalize the molecular interactions and binding modes of the designed compounds in the most relevant protein targets were carried out. Furthermore, in order to obtain information on the structure-activity relationship of the synthesized series, a 3-D-QSAR CoMFA and CoMSIA study was conducted and validated internally and externally (q2 = 0.625, 0.523 for CoMFA and CoMSIA and r2ncv = 0.967, 0.959 for CoMFA and CoMSIA, respectively).
Alarcón-Espósito, Jazmín,Araya-Maturana, Ramiro,Cabezas, David,Cerda-Cavieres, Christopher,Chung, Hery,Iturriaga-Vásquez, Patricio,Mella-Raipán, Jaime,Ojeda-Gómez, Claudia,Pessoa-Mahana, Carlos D.,Pessoa-Mahana, Hernán,Quiroz, Gabriel,Reyes-Parada, Miguel,Rodríguez-Lavado, Julio,Saitz, Claudio
(2020/10/18)

Receptor-interacting protein kinase 2 (RIPK2) and nucleotide-binding oligomerization domain (NOD) cell signaling inhibitors based on a 3,5-diphenyl-2-aminopyridine scaffold
Receptor-interacting protein kinase 2 (RIPK2) is a key mediator of nucleotide-binding oligomerization domain (NOD) cell signaling that has been implicated in various chronic inflammatory conditions. A new class of RIPK2 kinase/NOD signaling inhibitors bas
Suebsuwong, Chalada,Dai, Bing,Pinkas, Daniel M.,Duddupudi, Anantha Lakshmi,Li, Li,Bufton, Joshua C.,Schlicher, Lisa,Gyrd-Hansen, Mads,Hu, Ming,Bullock, Alex N.,Degterev, Alexei,Cuny, Gregory D.
supporting information

(2020/06/08)

COMPOSITIONS FOR USE IN METHODS OF INHIBITING PROTEIN KINASES
Identified compounds demonstrate protein kinase inhibitory activity and inhibition of dependent cell signaling pathways, such as NOD2 cell signaling. More specifically, the compounds are demonstrated to inhibit receptor interacting kinase 2 (RIPK2) and/or Activin- like kinase 2 (ALK2). Compounds that are either dual RIPK2/ALK2 inhibitors or that preferentially inhibit RIPK2 or ALK2 could provide therapeutic benefit.
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Paragraph 0006; 0008; 0017;0106; 0107

(2018/10/25)

GLUTATHIONE-DETECTING FLUORESCENT PROBE
[Problem] To provide the following: a novel fluorescent probe for detecting a compound, such as glutathione, that contains a —SH group; a detection method using said fluorescent probe; and a detection kit containing said probe. [Solution] A fluorescent pr
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Paragraph 0132; 0133; 0134

(2017/04/11)

N-sulfonylated tetrahydroquinolines and related bicyclic compounds for inhibition of RORγ activity and the treatment of disease
The invention provides tetrahydroquinoline and related compounds, pharmaceutical compositions, methods of inhibiting RORγ activity, reducing the amount of IL-17 in a subject, and treating immune disorders and inflammatory disorders using such tetrahydroqu
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Page/Page column 233; 234

(2016/12/26)

Burton's tyrosine kinase inhibitor
The invention provides a Burton's tyrosine kinase inhibitor. Particularly, a compound capable of serving as the Btk inhibitor is obtained through a wide and thorough research. It is shown through experimental results that the compound has a good inhibitin
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Paragraph 0118; 0119; 0120

(2017/01/17)

PHOSPHOINOSITIDE 3-KINASE INHIBITORS WITH ZINC BINDING MOIETY
PROBLEM TO BE SOLVED: To provide phosphoinositide 3-kinase inhibitors with a zinc binding moiety. SOLUTION: There is provided a compound represented by formula (I) in the figure. (X is S, O or the like; Y is CH, N or the like; G1 is optionally substituted N or the like; R1 and R2 are each independently H or the like; C is a substituted heterocycle or the like; B is a linear alkyl or the like; Ra and Rb together with the nitrogen atom coupled to them are morpholino or the like; G2 is an indazole ring or the like; q, r and s are independently from 0 to 1, provided that at least one of them is 1; t is from 0 to 1; n is from 0 to 4; and p is from 0 to 2.) COPYRIGHT: (C)2016,JPOandINPIT
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Paragraph 0487

(2016/10/07)

MK2 INHIBITORS AND USES THEREOF
The present invention provides compounds, compositions thereof, and methods of using the same.
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Paragraph 00945

(2014/10/03)

TREATMENT OF CANCERS HAVING K-RAS MUTATIONS
The present invention provides a method of treating a cancer associated with a K-ras mutation in a subject in need thereof. The method comprises the steps of: (1) identifying a subject with a cancer associated with a K-ras mutation; and (2) administering to the subject (i) an inhibitor of PI3 kinase and (ii) an HDAC inhibitor, wherein the PI3 kinase inhibitor and the HDAC inhibitor are administered in amounts which together are therapeutically effective.
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Paragraph 0574

(2013/05/08)

TREATMENT OF CANCERS HAVING K-RAS MUTATIONS
The present invention provides a method of treating a cancer associated with a K- ras mutation in a subject in need thereof. The method comprises the steps of (1) identifying a subject with a cancer associated with a K-ras mutation; and (2) adminsiterign to the subject (i) an inhibitor of PI3 kinase and (ii) an HDAC inhibitor, wherein the PI3 kinase inhibitor and the HDAC inhibitor are administered in amounts which together are therapeutically effective.
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Page/Page column 227

(2011/11/01)

FUSED HETEROCYCLIC C-GLYCOSIDES FOR THE TREATMENT OF DIABETES
The present invention provides compounds of Formula (IA) wherein A is selected from Formula (II) which have an inhibitory effect on the sodium dependent glucose transporter SGLT and their use in the treatment of diabetes.
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Page/Page column 52

(2010/11/18)

FUSED THIAZOLE AND THIOPHENE DERIVATIVES AS KINASE INHIBITORS
A series of fused bicyclic thiazole and thiophene derivatives which are substituted in the 2-position by an optionally substituted morpholin-4-yl moiety, and in the 4-position by hydroxy, oxo or an amine moiety, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions. (I)
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Page/Page column 97-98

(2009/07/17)

PYRROLOTHIAZOLES AS PI3-KINASE INHIBITORS
A series of 4,5-dihydro-6H-pyrrolo[3,4-d][1,3]thiazol-6-one derivatives, and analogues thereof, which are substituted in the 2-position by an optionally substituted morpholin-4-yl moiety, being selective inhibitors of PI3 kinase enzymes, are accordingly o
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Page/Page column 73

(2009/07/17)

TRICYCLIC KINASE INHIBITORS
A series of fused tricyclic thiazole and thiophene derivatives which are substituted in the 2-position of the thiazole or thiophene ring by an optionally substituted morpholin-4-yl moiety, being selective inhibitors of PI3 kinase enzymes, are accordingly
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Page/Page column 103-104

(2009/07/17)

PYRIDOSULFONAMIDE DERIVATIVES AS PI3 KINASE INHIBITORS
Invented is a method of inhibiting the activity/function of PB kinases using pyridosulfonamide derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of pyridosulfonamide derivatives.
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Page/Page column 69-70

(2009/05/30)

FUSED THIAZOLE DERIVATIVES AS KINASE INHIBITORS
A series of 5,5-dimethyl-5,6-dihydro-1,3-benzothiazol-7(4H)-one and 7,7-dimethyl-5,6,7,8-tetrahydro-4H-[1,3]thiazolo[5,4-c]azepin-4-one derivatives, and analogues thereof, which are substituted in the 2-position by an optionally substituted benzofused mor
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Page/Page column 29

(2008/06/13)

THIAZOLE DERIVATIVES AS KINASE INHIBITORS
A series of thiazole derivatives which are substituted in the 2-position by a substituted morpholin-4-yl moiety, being selective inhibitors of P13 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.
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Page/Page column 50-51

(2008/12/05)

Achieving multi-isoform PI3K inhibition in a series of substituted 3,4-dihydro-2H-benzo[1,4]oxazines
The SAR and pharmacokinetic profiles of a series of multi-isoform PI3K inhibitors based on a 3,4-dihydro-2H-benzo[1,4]oxazine scaffold are disclosed.
Perry, Benjamin,Alexander, Rikki,Bennett, Gavin,Buckley, George,Ceska, Tom,Crabbe, Tom,Dale, Verity,Gowers, Lewis,Horsley, Helen,James, Lynwen,Jenkins, Kerry,Crepy, Karen,Kulisa, Claire,Lightfoot, Helen,Lock, Chris,Mack, Stephen,Morgan, Trevor,Nicolas, Anne-Lise,Pitt, Will,Sabin, Verity,Wright, Sara
scheme or table
p. 4700 - 4704
(2009/04/08)

Improved P1/P1' substituents for cyclic urea based HIV-1 protease inhibitors: Synthesis, structure-activity relationship, and X-ray crystal structure analysis
We present several novel P1/P1' substituents that can replace the characteristic benzyl P1/P1' moiety of the cyclic urea based HIV protease inhibitor series. These substituents typically provide 5-10-fold improvements in binding affinity compared to the unsubstituted benzyl analogs. The best substituent was the 3,4-(ethylenedioxy)benzyl group. Proper balancing of the molecule's lipophilicity facilitated the transfer of this improved binding affinity into a superior cellular antiviral activity profile. Several analogs were evaluated further for protein binding and resistance liabilities. Compound 18 (IC90 = 8.7 nM) was chosen for oral bioavailability studies based on its log P and solubility profile. A 10 mg/kg dose in dogs provided modest bioavailability with C(max) = 0.22 μg/mL. X-ray crystallographic analysis of two analogs revealed several interesting features responsible for the 3,4-(ethylenedioxy)benzyl-substituted analog's potency: (1) Comparing the two complexes revealed two distinct binding modes for each P1/P1' substituent; (2) The ethylenedioxy moieties are within 3.6 A? of Pro 81 providing additional van der Waals contacts missing from the parent structure; (3) The enzyme's Arg 8 side chain moves away from the P1 substituent to accommodate the increased steric volume while maintaining a favorable hydrogen bond distance between the para oxygen substituent and the guanidine NH.
Nugiel, David A.,Jacobs, Kim,Cornelius, Lyndon,Chang, Chong-Hwan,Jadhav, Prabhakar K.,Holler, Edward R.,Klabe, Ronald M.,Bacheler, Lee T.,Cordova, Beverly,Garber, Sena,Reid, Carol,Logue, Kelly A.,Gorey-Feret, Lorraine J.,Lam, Gilbert N.,Erickson-Viitanen, Susan,Seitz, Steven P.
p. 1465 - 1474
(2007/10/03)