5 Crl:CD BR rats per sex per group received a single dose of (14)C- Imazapic (CL 263,222) by oral gavage or intravenous injection at 10 or 1000 mg/kg. One group received 14 consecutive non-radiolabelled daily oral doses followed by one (14)C labelled oral dose (10 mg/kg). After dosing with radiolabel, animals were housed in individual metabolism cages and sacrificed 7 days later.... Metabolites designated CL 303,459 and CL 263,284 ... and several minor radioactive components were also detected in small amounts (< 5% combined of the total radioactivity in the sample). In feces, metabolites CL 303,459 (4.29% (males) to 5.38% (females) of radioactivity in the sample), CL 263,284 (1.96% (males) and 0.85% (females)), and CL 290,610 (0.69% (males) and 0.70% (females)) were detected. The absolute amount of each of these corresponded to <0.2% of the administered dose. Several unknown metabolites accounted for less than 6% of total radioactivity in feces samples. The proposed metabolic pathway of (14)C- Imazapic ... was based on components identified in the excreta. Oxidation of the methyl group on the pyridine ring of (14)C- Imazapic produced metabolite CL 263,284. The presence of CL 303,459 suggested the initial step of ring closure, reduction to intermediate CL 280,442, followed by hydrolysis to CL 303,459 and further hydrolysis to CL 290,610.
来源:Hazardous Substances Data Bank (HSDB)
毒理性
致癌物分类
对人类不具有致癌性（未被国际癌症研究机构IARC列名）。
No indication of carcinogenicity to humans (not listed by IARC).
/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"，最小流量/。如果出现低血容量的迹象，使用0.9%的生理盐水（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/
/LABORATORY ANIMALS: Subchronic or Prechronic Exposure/ Imazapic (AC 263,222, purity: 93.7%) was mixed with saline and the resulting slurry was applied to the clipped skin of 6 New Zealand White rabbits/sex/dose at dose levels of 0 (saline), 250, 500, or 1000 mg/kg/day for 6 hrs/day 5 days/week for 3 consecutive weeks using an occlusive dressing. No mortalities occurred. No treatment-related clinical signs were observed. No skin irritation was observed at the treatment sites. No effect on body weight was observed. Hematological and clinical chemistry investigations revealed no effects of biological significance. No effect on mean relative organ weights was observed. Macroscopic and microscopic examinations revealed no treatment-related abnormalities. ... NOEL (M/F, systemic and skin) = 1000 mg/kg/day based on no treatment-related effects at the highest dose tested.
来源:Hazardous Substances Data Bank (HSDB)
吸收、分配和排泄
Imazapic在动物体内不会生物累积；如果摄入，会通过尿液和粪便迅速排出。
Imazapic does not bioaccumulate in animals; if ingested, then rapidly excreted through urine and feces.
5 Crl:CD BR rats/sex/group received a single dose of (14)C- Imazapic (CL 263,222) by oral gavage or intravenous injection at 10 or 1000 mg/kg. One group received 14 consecutive non-radiolabelled daily oral doses followed by one (14)C labelled oral dose (10 mg/kg). After dosing with radiolabel, animals were housed in individual metabolism cages and sacrificed 7 days later. Feces, urine, cage wash/rinse, cage wipes (methanol extracted), blood, fat, heart, spleen, ovaries, uterus, bone (femur), brain, kidney, liver, lungs, muscle (thigh), testes, and the residual carcass were analyzed for radioactivity by liquid scintillation counting (LSC). Metabolite profiles in urine, dissolved urine precipitate, and feces extract (ethyl ether) were determined using thin-layer chromatography (TLC) and high-performance liquid chromatography (HPLC). The major elimination route for dosed radioactivity was in urine. The mean percent of total dose (including cage wash and cage wipe) ranged from 94.0% to 102% (males) and 94.5% to 102% (females). The mean percent of total dose excreted in feces ranged from 0.79% to 3.44% (males) and 0.59% to 3.50% (females). The majority of radioactivity was excreted during 6 hours post-dosing. Mean radioactivity concentrations in blood 7 days after a single dose at 10 mg/kg were not detectable. At 1000 mg/kg, concentrations were 0.127 ppm for males and <0.1 ppm for females. Mean radioactivity concentrations in tissues were generally not detectable (<0.01 ppm) at 10 and 1000 mg/kg. Residual radioactivity in the carcass ranged from <0.001 ppm to 0.043 ppm. The unchanged test article, (14)C- Imazapic, accounted for >/= 93.5% and >/= 65.9% of the total radioactivity in urine (94% to 102% of total administered dose) and feces (0.59% to 3.50% of total administered dose) 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] INSECTICIDAL TRIAZINONE DERIVATIVES<br/>[FR] DÉRIVÉS DE TRIAZINONE INSECTICIDES
申请人：SYNGENTA PARTICIPATIONS AG
公开号：WO2013079350A1
公开（公告）日：2013-06-06
Compounds of the formula (I) or (I'), wherein the substituents are as defined in claim 1, are useful as pesticides.
式(I)或(I')的化合物，其中取代基如权利要求1所定义的那样，可用作杀虫剂。
[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.
