间三氟甲基苯乙酮置于吡啶,二氯化二硫体系中,化学反应 20.0H,以76%的收率获得3-(三氟甲基)苯甲酰氯 参考文献: Method For Preparation Of Carboxylic Acid Chlorides From Methyl Ketones[fr] Procédé De Préparation De Chlorures D'Acides Carboxyliques à Partir De Méthyl Cétones 标题: Method For Preparation Of Carboxylic Acid Chlorides From Methyl Ketones[fr] Procédé De Préparation De Chlorures D'Acides Carboxyliques à Partir De Méthyl Cétones 摘要:该发明揭示了一种从甲基酮开始制备羧酸氯化物的方法,该方法使用硫氯化物.
专利号:WO-2021038419-A1 优先权日:2019-08-23 标题 :Kinase inhibitors and methods of synthesis and treatment 发明人:ZAVORONKOVS ALEKSANDRS; IVANENKOV YAN; POLYKOVSKIY DANIIL; ALIPER ALEKSANDR 权利人:INSILICO MEDICINE IP LTD 摘要:Compounds that function as kinase inhibitors are provided. The kinase inhibitors can have any structure of the formulae provided herein, such as shown for Compounds 1-4. A pharmaceutical composition can include: the compound of one of the embodiments; and a pharmaceutically acceptable carrier having the compound. A method of inhibiting a kinase can include: providing the compound of one of the embodiments described herein to the kinase such that the kinase is inhibited. The methods can include inhibiting DDR1 and/or DDR2, and thereby providing a modulation or decrease in the activity of DDR1 and/or DDR2. This decrease in DDR1 and/or DDR2 activity can be used as therapy to treat conditions related to DDR1 and/or DDR2 activity, such as fibrosis, cancer, and others.
专利号:US-4244970-A 优先权日:1979-12-20 标题:Method of treating inflammation 发明人:DEWHIRST FLOYD E 权利人:FORSYTH DENTAL INFIRMARY 摘要:A method of treating inflammation and inhibiting prostaglandin synthesis employing 2-hydroxybenzophenone and substituted 2-hydroxybenzophenones.
专利号:US-8372971-B2 优先权日:2004-08-25 标 题:Heterocyclic compounds and methods of use 发明人:WRASIDLO WOLFGANG; DNEPROVSKAIA ELENA 权利人:TARGEGEN INC; WRASIDLO WOLFGANG; DNEPROVSKAIA ELENA 摘要:Heterocyclic compounds derived from benzotriazine, triazines, triazoles and oxadiazoles are disclosed. The methods of synthesis and of use of such heterocyclic compounds are also provided.
专利号:US-2008096883-A1 优先权日:2004-08-11 标题 :Trifluoromethyl substituted benzamides as kinase inhibitors 发明人:CARAVATTI GIORGIO; FURET PASCAL; IMBACH PATRICIA; MARTINY-BARON GEORG; PEREZ LAWRENCE BLAS; SHENG TAO 权利人:CARAVATTI GIORGIO; FURET PASCAL; IMBACH PATRICIA; MARTINY-BARON GEORG; PEREZ LAWRENCE BLAS; SHENG TAO 摘要:The invention relates to trifluoromethyl substituted benzamide compounds of the formula (I), pharmaceuticals comprising these compounds, their use as or for the manufacture of pharmaceuticals, particularly as inhibitors of protein kinases and/or the treatment of a condition, disorder or disease state mediated by a protein kinase activity and/or a proliferative disease, methods of treatment comprising administering the compounds, especially of therapeutic and prophylactic treatment, methods for the manufacture of the compounds and novel intermediates and partial steps for their synthesis.
专利号:US-9695191-B2 优先权日:2009-08-05 标题 :Conformationally constrained, fully synthetic macrocyclic compounds 发明人:OBRECHT DANIEL; ERMERT PHILIPP; OUMOUCH SAID; LACH FRANCK; LUTHER ANATOL; MARX KARSTEN; MÖHLE KERSTIN 权利人:OBRECHT DANIEL; ERMERT PHILIPP; OUMOUCH SAID; LACH FRANCK; LUTHER ANATOL; MARX KARSTEN; MÖHLE KERSTIN; POLYPHOR AG 摘要:Conformationally restricted, spatially defined 12-30 membered macrocyclic ring systems of type (I) are constituted by three distinct building blocks: an aromatic template a, a conformation modulator b and a spacer moiety c as detailed in the description and the claims. Macrocycles of type (I) are readily manufactured by parallel synthesis or combinatorial chemistry. They are designed to interact with specific biological targets. In particular, they show agonistic or antagonistic activity on the motilin receptor (MR receptor), on the serotonin receptor of subtype 5-HT 2B (5-HT 2B receptor), and on the prostaglandin F2•receptor (FP receptor). They are thus potentially useful for the treatment of hypomotility disorders of the gastrointestinal tract such as diabetic gastroparesis and constipation type irritable bowl syndrome; of CNS related diseases like migraine, schizophrenia, psychosis or depression; of ocular hypertension such as associated with glaucoma and preterm labour.
专利号:US-9745253-B2 优先权日:2015-03-13 标 题 :Alpha-cinnamide compounds and compositions as HDAC8 inhibitors 发明人:BAIR KENNETH W; Barczak Nicholas; HAN BINGSONG; LANCIA JR DAVID R; LIU CUIXIAN; MARTIN MATTHEW W; NG PUI YEE; Rudnitskaya Aleksandra; THOMASON JENNIFER R; ZABLOCKI MARY MARGARET; ZHENG XIAOZHANG 权利人:FORMA THERAPEUTICS INC 摘要:The present invention relates to inhibitors of histone deacetylases, in particular HDAC8, that are useful for the treatment of cancer and other diseases and disorders, as well as the synthesis and applications of said inhibitors.
摘要:Davies, G. H. M.; Wisniewski, S. R., Science of Synthesis Knowledge Updates, (2021) 2, 214. 摘要:Aitken, R. A., Science of Synthesis Knowledge Updates, (2022) 2, 39. 摘要:Li, D.-D.; Wang, G.-W., Science of Synthesis: Catalytic Transformations via CH Activation, (2015) 2, 375.