CAS: 417716-92-8; 4-(3-Chloro-4-(3-Cyclopropylureido)Phenoxy)-7-Methoxyquinoline-6-Carboxamide

上下游产品

CAS号417722-95-3 Phenyl N-(4-(6-... | CAS号765-30-0 环丙胺 | CAS号857890-39-2 乐伐替尼甲磺酸盐

4-氨基水杨酸置于草酰氯,四丁基溴化铵,Potassium Carbonate,N,N-二甲基甲酰胺,原甲酸三乙酯,Potassium Hydroxide体系中,用 二苯醚,联苯,二氯甲烷,二甲基亚砜,丙酮,叔丁醇 作为反应溶剂,化学反应 23.08H,反应生成 乐伐替尼
参考文献:一种合成乐伐替尼的方法
标题:一种合成乐伐替尼的方法
摘要:本发明属于化学制药领域,具体涉及一种合成乐伐替尼的方法,包括以下步骤:步骤1,以4‑氨基水杨酸为原料,经甲基化,与麦氏酸缩合,高温环合,氯代,氨化,得到4‑氯‑7‑甲氧基喹啉‑6‑甲酰胺;步骤2,以3‑氯‑4‑氨基苯酚为原料,经与氯甲酸苯酯及环丙胺反应得到1‑(2‑氯‑4‑羟基苯基)‑3‑环丙基脲;步骤3,将步骤1制得的4‑氯‑7‑甲氧基喹啉‑6‑甲酰胺和步骤2制得的1‑(2‑氯‑4‑羟基苯基)‑3‑环丙基脲在叔丁醇钾的作用下反应得到乐伐替尼;本发明提供了一种合成乐伐替尼的全新路线.所用试剂便宜易得,操作简单,而且产率比其他方法高,而且易于工业化生产.

专利信息

专利号:US-2022233673-A1
优先权日:2019-06-04
标 题:METHODS OF PRODUCING SHIGA TOXIN B-SUBUNIT (STxB) MONOMERS AND OLIGOMERS, AND USES THEREOF
发明人：BILLET ANNE; SCHMIDT FRÉDÉRIC; JOHANNES LUDGER; SERVENT DENIS; MOURIER GILLES; TARTOUR ÉRIC; KAY MICHAEL; FULCHER JAMES M
权利人:INST CURIE; CENTRE NAT RECH SCIENT; INST NAT SANTE RECH MED; COMMISSARIAT A LENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES CEA; APHP ASSIST PUBLIQUE HOPITAUX DE PARIS; UNIV PARIS; UNIV OF UTAH RESEARCH FOUDATION; UNIV UTAH RES FOUND
摘要:A method of producing a monomer of a Shiga toxin B-subunit (STxB) protein or of a variant thereof by peptide chemical synthesis, as well as to a method of producing a pentamer of the STxB protein or of the variant thereof. The methods are particularly advantageous as they overcome major issues typically observed in peptide chemical synthesis, including solubility and purity issues.

专利号:US-2022118123-A1
优先权日:2019-02-22
标 题 :Combination of ar antagonists and targeted thorium conjugates
发明人：HAMMER STEFANIE; HAGEMANN URS BEAT; HAENDLER BERNARD; LEJEUNE PASCALE; ZITZMANN-KOLBE SABINE; SCHATZ CHRISTOPH; KARLSSON JENNY
权利人:BAYER AG; BAYER AS
摘要:The present invention covers combinations of at least two components, component A and component B, comprising component A being PSMA-TTC, and component B being an antiandrogen selected form AR antagonists such as from cyproterone acetate, bicalutamide, flutamide, nilutamide, enzalutamide, apalutamide, darolutamide or keto-darolutamide, or an AR degrader such as ARV-110, or an ARN-terminal domain binder such as EPI-506, or an antisense oligonucleotide that reduces AR expression such as EZN-4176 or AZD-5312, or an androgen synthesis inhibitor such as abiraterone, particularly abiraterone acetate, seviteronel, galeterone, orteronel or ketoconazole, or a dual AR antagonist and androgen synthesis inhibitor such as ODM-204. Another aspect of the present invention covers the use of such combinations as described herein for the preparation of a medicament for the treatment or prophylaxis of a disease, particularly for the treatment of a hyper-proliferative disease.

专利号:US-2024360247-A1
优先权日:2021-08-10
标 题:Compositions and methods for treatment of cancer
发明人：CHATTERJEE SUBROTO
权利人:UNIV JOHNS HOPKINS
摘要:Compositions in the prevention and treatment of cancers, such as colorectal cancer or diseases associated with abnormal levels of β-1,4-galactosyltransferase-V (β-1,4-GalT-V), include at least one inhibitor of glycosphingolipid synthesis.

专利号:US-12390420-B1
优先权日:2024-10-22
标题 :Compositions for targeted delivery of therapeutic agents and methods for the synthesis and use thereof
发明人：EGUCHI MASAKATSU
权利人:BRYET US INC
摘要:The present disclosure provides compositions and methods for delivering therapeutic agents to particular tissues or cells in a subject. The composition disclosed herein combines unique properties of porous micro- or nano-particles with host-guest chemistry provided by functionalized silicon particle, offering a versatile approach to addressing the challenges associated with delivering therapeutic agents to target tissues or sites within the body. The present disclosure also provides a method for synthesizing a composition capable of delivering therapeutic agents to particular tissues or cells in a subject.

专利号:US-12180228-B2
优先权日:2019-06-05
标题:Compounds, conjugates, and compositions of epipolythiodiketopiperazines and polythiodiketopiperazines and uses thereof
发明人：MOVASSAGHI MOHAMMAD; OLSSON CHASE ROBERT; SCOTT TONY Z; CHEAH JAIME; PAYETTE JOSHUA NATHANIEL
权利人:MASSACHUSETTS INST TECHNOLOGY
摘要:The present disclosure provides, e.g., compounds, compositions, kits, methods of synthesis, and methods of use, involving epipolythiodiketopiperazines and polythiodiketopiperazines.

专利号:US-2025162973-A1
优先权日:2022-02-22
标题:Methods of synthesis and uses of agrimol compounds
发明人：CHE CHI MING; FU ZHIWEN; LEUNG YIU CHUNG GULICE
权利人:VERSITECH LTD; LABORATORY FOR SYNTHETIC CHEMISTRY AND CHEMICAL BIOLOGY LTD
摘要:Synthetic agrimol B and derivatives thereof (“compoundsâ€?) that have anticancer properties are disclosed. Methods for synthesizing the compounds with an overall yield ≥7% are disclosed. Pharmaceutical formulations in forms suitable for the delivery of the compounds to a subject in need thereof are disclosed. Methods of using the compounds for treating a cancer, reducing a cancer, or treating or ameliorating one or more symptoms associated with a cancer, such as non-small-cell lung cancer, in a subject are also disclosed. The methods include (i) administering to the subject the pharmaceutical formulation containing one or more compounds, for one or more times. The compounds can selectively kill cancer cells and/or cancer stem cells over noncancerous cells by inducing mitochondria dysfunction and/or inhibiting ER to Golgi trafficking in the cancer cells and/or cancer stem cells.