CAS: 485-49-4; (R)-6-((S)-6-Methyl-5,6,7,8-Tetrahydro-[1,3]Dioxolo[4,5-G]Isoquinolin-5-yl)-[1,3]Dioxolo[4,5-E]Isobenzofuran-8(6H)-One

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CAS号50-00-0 甲醛 | CAS号56083-00-2 (+)-bicuculline | CAS号64395-07-9 Furo[3,4-e]-1,3... | CAS号58343-48-9 5-formyl-1,3-be... | CAS号185022-35-9 N-(2-(benzo[d][... | CAS号40709-69-1 (-)-双环甲硫脲

📜5-Formyl-Benzo[1,3]Dioxole-4-Carboxylic Acid置于盐酸,Sodium Hydroxide,Sodium Tetrahydroborate,甲酸,氯化亚砜,硫酸,溶剂黄146,三氯氧磷体系中,用 二氯甲烷,苯 作为反应溶剂,化学反应 15.25H,反应生成 (+)-荷包牡丹碱
参考文献:双瓜氨酸和去甲胆碱对映异构体的合成,抗gaba活性和优选构象.
标题:双瓜氨酸和去甲胆碱对映异构体的合成,抗gaba活性和优选构象.
摘要:使用bischler-Napieralski环化作为关键步骤,从胡椒醛中合成了赤型-(+/-)-[1Sr,9Rs]-核苷和苏型-(+/-)-[1Sr,9Sr]-去甲rad啶.拆分产生对映体纯度> 99.5%的(+)-[1S,9R]-冰核碱([1S,9R] Norbic)和(-)-[1R,9S]-冰核碱([1R,9S] Norbic).通过将后面的产物甲基化,可以容易地获得双瓜氨酸对映异构体.作为抑制gaba(a)受体结合的抑制剂,[1S,9R] Bic的效力比[1R,9S] Bic的效力高约70倍,在ph 7.1和5.0时,[1S,9R] Bic的效力比[1S,9R] Norbic约高100到900倍分别.同样,[1S,9R] Norbic作为[1S,9R] Bic作为gaba特异性(36)cl(-)离子通量的抑制剂的效力要低得多.观测到[1S中,由n2-Ch(3)取代引起的体外生物活性增加了大约两个数量级,
DOI:10.1016/0223-5234(96)83969-9

专利信息

专利号:US-2022160788-A1
优先权日:2019-03-22
标题 :Bifunctional vectors allowing bcl11a silencing and expression of an anti-sickling hbb and uses thereof for gene therapy of b-hemoglobinopathies
发明人：MICCIO ANNARITA; AMENDOLA MARIO; BRUSSON MÉGANE; CAVAZZANA MARINA; MAVILIO FULVIO
权利人:INST NAT SANTE RECH MED; UNIV DEVRY VAL DESSONNE; ASSIST PUBLIQUE HOPITAUX PARIS APHP; UNIV PARIS; FOND IMAGINE
摘要:The #β-hemoglobinopathies #β-thalassemia (BT) and sickle cell disease (SCD) are the most frequent genetic disorders worldwide. These diseases are caused by mutations causing reduced or abnormal synthesis of the β-globin chain of the adult hemoglobin (Hb) tetramer. Here, the inventors intend to improve HSC-based gene therapy for β-thalassemia and SCD by developing an innovative, highly infectious LV vector expressing a potent anti-sickling β-globin transgene and a second biological function either increasing fetal γ-globin expression (for β-thalassemia and SCD). More particularly, the inventors have designed a novel lentivirus (LV), which carry two different functions: βAS3 gene addition and gene silencing. This last strategy allows the re-expression of the fetal γ-globin genes (HBG1 and HBG2) and production of the endogenous fetal hemoglobin (HbF). Elevated levels of HbF and HbAS3 (Hb tetramer containing βAS3-globin) will benefit the β-hemoglobinopathy phenotype by increasing the total amount of β-like globin that will: (i) reduce the alpha precipitates and improve the alpha/non alpha ratio in β-thalassemia, and (ii) reduce the sickling in SCD. This combined strategy will improve the β-hemoglobinopathy phenotype at a lower vector copy number (VCN) per cell compared to a LV expressing the βAS3 alone.

专利号:US-6409988-B1
优先权日:1999-07-01
标 题:Radiolabeled 1-aryl pyrazoles, the synthesis thereof and the use thereof as pest GABA receptor ligands
发明人：DHANOA DALJIT S; MEEGALLA SANATH; DOLLER DARIO; SOLL RICHARD M
权利人:DIMENSIONAL PHARM INC
摘要:The present invention is directed to radiolabeled compounds of Formula I:or salts thereof, whereR1 represents R8, R8O, R8SO2, R8SO or R8S in which R8 is tritiated or deuterated methyl;X is halo, cyano, C1-6 alkoxycarbonyl, C2-6 alkynyl, optionally substitutedC6-14 aryl or an optionally substituted 5- to 7-membered heteroaromatic ring linked to thiazole via a carbon-carbon bond;R2 is hydrogen or amino; andR3-R7 are defined in the specification.The invention is also directed to methods of using such compounds for demonstrating specific insect GABA receptors, qualitatively screening for compounds acting on an insect GABA receptor or quantitatively assaying concentrations of a compound acting on an insect GABA receptor.

专利号:US-2006287397-A1
优先权日:2002-04-26
标 题:Dl-hydroxy-alkyl-phenylamides having anticonvulsive activity
发明人：MEZA TOLEDO SERGIO E
权利人:MEZA TOLEDO SERGIO E
摘要:New anticonvulsant compounds were synthesized and they include the compounds: DL-2-hydroxy-2-(3′,5′-bistrifluoromethylphenyl)butyramide, DL-2-hydroxy-2-(4′-trifluoromethylphenyl)butyramide, DL-2-hydroxy-2-(3′,4′-dichlorophenyl)butyramide, DL-2-hydroxy-2-(3′-bromophenyl)butyramide, DL-2-hydroxy-2-(4′-bromophenyl)butyramide, DL-2-hydroxy-2-(3′-nitrophenyl)butyramide, DL-3-hydroxy-3-(3′,4′-dichlorophenyl)pentanamide, DL-3-hydroxy-3-(4′-bromophenyl)pentanamide, DL-4-hydroxy-4-(3′,4′-dichlorophenyl) hexanamide and DL-4-hydroxy-4-(4′-bromophenyl)hexanamide. They have a significant anticonvulsant activity against pentylenetetrazol-induced seizures as well as unexpected differences in anticonvulsant activity respect those of the non-halogenated compounds. The invention further provides methods for the synthesis of the DL-hydroxy-alkyl-phenyl amides as exemplified in the examples.

专利号:WO-0040532-A2
优先权日:1998-12-31
标 题:Synthesis of dihydrohonokiol compositions

专利号:US-6518266-B1
优先权日:1999-07-22
标题:1- Aryl-3-thioalkyl pyrazoles, the synthesis thereof and the use thereof as insecticides
发明人：DHANOA DALJIT S; DOLLER DARIO; MEEGALLA SANATH; SOLL RICHARD M; WISNEWSKI NANCY; SILVER GARY; STINCHCOMB DAN T; SEWARD R LEE; AGRAFIOTIS DIMITRIS; SHA DEYOU
权利人:DIMENSIONAL PHARMACEUTICALS 3; HESKA CORP
摘要:The present invention is directed to novel pyrazole derivatives and their use as pesticidal agents. The pyrazole derivatives have Formula I:or a salt thereof, whereR1 represents R5O, R5SO2, R5SO or R5S in which R5 is as defined herein;X is halo, cyano, C1-6 alkoxycarbonyl, C2-6 alkynyl, optionally substituted C6-14 aryl or an optionally substituted 5- to 7-membered heteroaromatic ring linked to thiazole via a carbon-carbon bond;R2 is hydrogen, amino, chloro, bromo, iodo, cyano, C1-6 alkoxy, C1-6 alkyl or C6-10 aryl; andR3-R7 each represent hydrogen, halogen, straight- or branched-chain C1-4 alkyl or C1-4 alkoxy, either of which is unsubstituted or substituted by one or more halogen atoms, straight- or branched-chain C1-4 alkylthio or C1-4 alkylsulphinyl, either of which is substituted by one or more halogen atoms, nitro, cyano, or straight- or branched-chain C1-4 alkylsulphonyl group which is unsubstituted or substituted by one or more halogen atoms.

专利号:US-6545033-B1
优先权日:1999-10-06
标 题:Fused 1-(2,6-dichloro-4-trifluoromethylphenyl)-pyrazoles, the synthesis thereof and the use thereof as pesticides
发明人：DHANOA DALJIT S; MEEGALLA SANATH; SOLL RICHARD M; DOLLER DARIO; SHA DEYOU; LIU RUIPING; SILVER GARY; LEE YU-KAI
权利人:DIMENSIONAL PHARM INC
摘要:The present invention is directed to novel pyrazole derivatives and their use as pesticidal agents. The pyrazole derivatives have Formula I:or a salt thereof, whereR1 is amino, hydrogen, alkyl, hydroxy, halo, alkoxy, alkylamino, dialkylamino, alkylthio, alkylsulfinyl, alkylsulfonyl, trifluoroalkylsulfinyl, trifluoroalkylsulfonyl, hydroxy, amino, trifluoromethyl, acetylamino, -OSO2R2, -OS(O)R2, -OC(O)R2, -OC(O)NHR2, or -NHC(O)NHR2 where R2 is C1-4 alkyl or optionally substituted aryl;X, Y and Z are each independently (CH)n, (CR3R4)n, S, S(O), or SO2, wherein n is 1-2, R3 and R4 are defined herein;Q is N or C-R6, wherein R6 is fluoro, chloro, bromo, or iodo;R5 is halo, C1-C6 alkyl, C1-C4 alkenyl, C1-C4 alkoxy, C1-C4 alkylamino, C1-C4 dialkylamino, C1-C4 alkylthio, C1-C4 alkylsulfinyl, C1-C4 alkylsulfonyl, C1-C4 trifluoroalkylsulfinyl, C1-C4 trifluoroalkylsulfonyl, hydroxy, amino, or trifluoromethyl; andwith the proviso that only one of X, Y and Z can be S, S(O) or SO2.