Solubility at 20 °C (w/w%): Acetone 1.2%; toluene 0.06%; at 25 °C (w/v%): acetic acid 0.67%
蒸汽压力:
1.81X10-10 mm Hg at 25 °C (est)
稳定性/保质期:
在常温常压下保持稳定,应避免与强氧化剂接触。
分解:
When heated to decomposition it emits toxic vapors of /sulfur oxides, nitrogen oxides and F-/.
解离常数:
pKa = 4.37
计算性质
辛醇/水分配系数(LogP):
2
重原子数:
27
可旋转键数:
5
环数:
2.0
sp3杂化的碳原子比例:
0.23
拓扑面积:
141
氢给体数:
2
氢受体数:
11
ADMET
代谢
一系列研究被进行以评估(14)C-SL-160(P)/flazasulfuron/在不同性别的大鼠(CRL: CD BR VAF/Plus)群体中的吸收、分布、代谢和排泄。在这些研究中,(14)C-SL-160(P)(CP-1385; 55.8 mCi/mMole; 放射性纯度报告为97.29%、97.5%、98.49%、99.2%和>98%)通过口服灌胃的方式给药,剂量为2或50 mg/kg或2 mg/kg。在/一项研究/中,大鼠在口服(14)C-SL-160(P)的第15天之前,已经连续14天接受非标记SL-160(Y-920205; 98.9%纯度)的口服灌胃剂量。在单次和重复剂量研究中,母体化合物是尿液(雄性:19-40%;雌性:51-67%的给药剂量)中的代谢物轮廓的主要成分,粪便中(雄性和雌性:2-5%的给药剂量)和胆汁中(雄性和雌性:0.6-2%的给药剂量)的量较少。在这些基质中,包括母体化合物在内,共检测到多达11个馏分。最常见的代谢物(以给药剂量的百分比表示)是HDTG+TPPG(在尿液中大约占6.5-12%,在粪便中大约占0.4-2%,在胆汁中大约占6.5-14%),其次是DTPU(N-(4,6-二甲氧基-2-嘧啶基)-N-[3-(三氟甲基)-2-吡啶基]脲)、HDPU、6-甲氧基-2-[[3-(三氟甲基)-2-吡啶基]氨基]-4-嘧啶醇、TPSA(3-三氟甲基)-2-吡啶磺酰胺)和MTMG,含量较少(<5%)。单独来看,未识别的馏分在尿液和胆汁代谢物轮廓中通常占给药剂量的不到2%。粪便代谢物轮廓中有高达35%的未识别馏分。
A series of studies were conducted to evaluate the absorption, distribution, metabolism, and excretion of (14)C-SL-160(P)/flazasulfuron/ in groups of 4 or 5 rats (CRL: CD BR VAF/Plus)/sex. In these studies, (14)C-SL-160(P) (CP-1385; 55.8 mCi/mMole; radiolabel purity variously reported as 97.29%, 97.5%. 98.49%., 99.2% and >98%) was administered orally by gavage at doses of 2 or 50 mg/kg or 2 mg/kg . In /one study/, rats had received daily oral gavage doses of nonlabeled SL-160 (Y-920205; 98.9% purity) for 14 days, prior to oral dosing with (14)C-SL-160(P) on Day 15. In the single and repeated dose studies, parent compound was the primary component in the metabolite profiles for urine (males: 19-40%; females: 51-67% of administered dose), with lesser amounts in feces (males and females: 2-5% of administered dose), and bile (males and females: 0.6-2% of administered dose). Including parent compound up to 11 fractions were detected among these matrices. The most prevalent metabolite (expressed as percent of administered dose) were HDTG+TPPG (approximately 6.5-12% in urine, approximately 0.4-2% in feces, and approximately 6.5-14% in bile), with minor amounts < 5%) of DTPU (N-(4,6-Dimethoxy-2-pyrimidinyl)-N-[3-(trifluoromethyl)-2-pyridinyl]urea), HDPU, 6-Methoxy-2-[[3-(trifluoromethyl)-2-pyridinyl]amino]-4-pyrimidinol, TPSA (3-Trifluoromethyl)-2-pyridinesulfonamide), and MTMG. Individually, unidentified fractions generally accounted for less than 2% of the administered dose in the urine and biliary metabolite profile. The fecal metabolite profile had up to 35% unidentified of the recovered dose.
/SRP:/ Immediate first aid: Ensure that adequate decontamination has been carried out. If patient is not breathing, start artificial respiration, preferably with a demand valve resuscitator, bag-valve-mask device, or pocket mask, as trained. Perform CPR if necessary. Immediately flush contaminated eyes with gently flowing water. Do not induce vomiting. If vomiting occurs, lean patient forward or place on the left side (head-down position, if possible) to maintain an open airway and prevent aspiration. Keep patient quiet and maintain normal body temperature. Obtain medical attention. /Poisons A and B/
/SRP:/ Basic treatment: Establish a patent airway (oropharyngeal or nasopharyngeal airway, if needed). Suction if necessary. Watch for signs of respiratory insufficiency and assist ventilations if needed. Administer oxygen by nonrebreather mask at 10 to 15 L/min. Monitor for pulmonary edema and treat if necessary ... . Monitor for shock and treat if necessary ... . Anticipate seizures and treat if necessary ... . For eye contamination, flush eyes immediately with water. Irrigate each eye continuously with 0.9% saline (NS) during transport ... . Do not use emetics. For ingestion, rinse mouth and administer 5 mL/kg up to 200 mL of water for dilution if the patient can swallow, has a strong gag reflex, and does not drool ... . Cover skin burns with dry sterile dressings after decontamination ... . /Poisons A and B/
来源:Hazardous Substances Data Bank (HSDB)
毒理性
解毒与急救
/SRP:/ 高级治疗:对于无意识、严重肺水肿或严重呼吸困难的病人,考虑进行口咽或鼻咽气管插管以控制气道。使用气囊面罩装置的正压通气技术可能有益。考虑使用药物治疗肺水肿……。对于严重的支气管痉挛,考虑给予β激动剂,如沙丁胺醇……。监测心率和必要时治疗心律失常……。开始静脉输注D5W /SRP: "保持开放",最低流量/。如果出现低血容量的迹象,使用0.9%生理盐水(NS)或乳酸林格氏液。对于伴有低血容量迹象的低血压,谨慎给予液体。注意液体过载的迹象……。使用地西泮或劳拉西泮治疗癫痫……。使用丙美卡因氢氯化物协助眼部冲洗……。 /Poisons A and B/
/SRP:/ Advanced treatment: Consider orotracheal or nasotracheal intubation for airway control in the patient who is unconscious, has severe pulmonary edema, or is in severe respiratory distress. Positive-pressure ventilation techniques with a bag valve mask device may be beneficial. Consider drug therapy for pulmonary edema ... . Consider administering a beta agonist such as albuterol for severe bronchospasm ... . Monitor cardiac rhythm and treat arrhythmias as necessary ... . Start IV administration of D5W /SRP: "To keep open", minimal flow rate/. Use 0.9% saline (NS) or lactated Ringer's if signs of hypovolemia are present. For hypotension with signs of hypovolemia, administer fluid cautiously. Watch for signs of fluid overload ... . Treat seizures with diazepam or lorazepam ... . Use proparacaine hydrochloride to assist eye irrigation ... . /Poisons A and B/
A series of studies were conducted to evaluate the absorption, distribution, metabolism, and excretion of (14)C-SL-160(P)/flazasulfuron/ in groups of 4 or 5 rats (CRL: CD BR VAF/Plus)/sex. In these studies, (14)C-SL-160(P) (CP-1385; 55.8 mCi/mMole; radiolabel purity variously reported as 97.29%, 97.5%. 98.49%., 99.2% and >98%) was administered orally by gavage at doses of 2 or 50 mg/kg or 2 mg/kg . In /one study/, rats had received daily oral gavage doses of nonlabeled SL-160 (Y-920205; 98.9% purity) for 14 days, prior to oral dosing with (14)C-SL-160(P) on Day 15. ... Differences were generally not noted between dose levels or between single versus repeated dose administration, but were noted between males and females. The studies demonstrated that 14C SL-160(P) is rapidly absorbed following a single oral dose of 2 or 50 mg/kg. By 48 hours post exposure, males and females absorbed 94% and 93% of the low dose, respectively, and 86% and 93% of the high dose, respectively. A similar pattern was observed when low- and high-dose animals were followed up to 168 hours with little difference noted between a single or repeated exposure. Elimination via the urine was the major route of excretion, accounting for 74-80% and 90-94% in males and females, respectively, following both low- and high-dose and single and repeated dose administration. Time course data revealed that a significant portion of the radioactivity in urine was excreted by 48-72 hours post exposure. Feces were the secondary route of elimination, accounting for 21-24% and 9-10% in males and females, respectively, following both low- and high-dose and single and repeated dose administration. The biliary excretion study determined that approximately 9.5% of the administered dose appeared in bile by 48 hours in low-dose males and females and high-dose females, with approximately 16.5% in high-dose males. Tissue distribution studies indicated that 14C-SL-160(P) is rapidly excreted from the system, with less than 4% (males) and 1% (females) of the administered radioactivity remaining in the tissues seven days after dosing. In general, the pattern of the radiolabel distribution in tissues was similar between the low- and high-dose groups in the single oral dose study and between the low-dose groups in the single and repeated dose groups. Pharmacokinetic studies confirmed the rapid absorption and elimination of 14C-SL-160(P). Following a single oral dose of (14)C-SL-160(P), tmax values (provided only for individual animals; mathematically determined value not provided) ranged from 30 minutes (3/5 animals/sex) or 4 hours (2/5 animals/sex) at 2 mg/kg, while the median tmax was 6 hours in males and 4 hours in females at the 50 mg/kg dose. At 2 and 50 mg/kg, males had slightly longer elimination half times for the blood than females (males: 27 and 36 hours, respectively; females: 18.8 and 33.8 hours, respectively). Likewise, males had a greater AUC (304 and 4440 ug-eq/g hr, respectively) than females (189 and 3080 ug-eq/g hr, respectively).
[EN] ACC INHIBITORS AND USES THEREOF<br/>[FR] INHIBITEURS DE L'ACC ET UTILISATIONS ASSOCIÉES
申请人:GILEAD APOLLO LLC
公开号:WO2017075056A1
公开(公告)日:2017-05-04
The present invention provides compounds I and II useful as inhibitors of Acetyl CoA Carboxylase (ACC), compositions thereof, and methods of using the same.
[EN] 3-[(HYDRAZONO)METHYL]-N-(TETRAZOL-5-YL)-BENZAMIDE AND 3-[(HYDRAZONO)METHYL]-N-(1,3,4-OXADIAZOL-2-YL)-BENZAMIDE DERIVATIVES AS HERBICIDES<br/>[FR] DÉRIVÉS DE 3-[(HYDRAZONO))MÉTHYL]-N-(TÉTRAZOL-5-YL)-BENZAMIDE ET DE 3-[(HYDRAZONO)MÉTHYL]-N-(1,3,4-OXADIAZOL-2-YL)-BENZAMIDE UTILISÉS EN TANT QU'HERBICIDES
申请人:SYNGENTA CROP PROTECTION AG
公开号:WO2021013969A1
公开(公告)日:2021-01-28
The present invention related to compounds of Formula (I): or an agronomically acceptable salt thereof, wherein Q, R2, R3, R4, R5 and R6 are as described herein. The invention further relates to compositions comprising said compounds, to methods of controlling weeds using said compositions, and to the use of compounds of Formula (I) as a herbicide.
[EN] HERBICIDALLY ACTIVE HETEROARYL-S?BSTIT?TED CYCLIC DIONES OR DERIVATIVES THEREOF<br/>[FR] DIONES CYCLIQUES SUBSTITUÉES PAR HÉTÉROARYLE À ACTIVITÉ HERBICIDE OU DÉRIVÉS DE CELLES-CI
申请人:SYNGENTA LTD
公开号:WO2011012862A1
公开(公告)日:2011-02-03
The invention relates to a compound of formula (I), which is suitable for use as a herbicide wherein G is hydrogen or an agriculturally acceptable metal, sulfonium, ammonium or latentiating group; Q is a unsubstituted or substituted C3-C8 saturated or mono-unsaturated heterocyclyl containing at least one heteroatom selected from O, N and S, or Q is heteroaryl or substituted heteroaryl; m is 1, 2 or 3; and Het is an optionally substituted monocyclic or bicyclic heteroaromatic ring; and wherein the compound is optionally an agronomically acceptable salt thereof.
The present invention provides triazole compounds useful as inhibitors of Acetyl CoA Carboxylase (ACC), compositions thereof, and methods of using the same.