CAS: 1912445-55-6; (S)-4-(3-(But-2-Ynamido)Piperidin-1-yl)-5-Fluoro-2,3-Dimethyl-1H-Indole-7-Carboxamide

上下游产品

4-Bromo-5-Fluoro-2,3-Dimethyl-1H-Indole-7-Carboxylic Acid 1912445-96-5

📜2-氨基-4,5-二氟苯甲酸甲酯置于磷酸二苯酯,Sodium Methylate,Potassium Hydrogencarbonate,Formamide,二苯基次膦酰氯体系中,用 醋酸异丙酯,二甲基亚砜,N,N-二甲基甲酰胺 用作溶剂,化学反应 24.0H,反应生成化合物bms-986195
参考文献:利用高通量实验推动药物路线发明:Branebrutinib (Bms-986195) 的四步商业合成
标题:利用高通量实验推动药物路线发明:Branebrutinib (Bms-986195) 的四步商业合成
摘要:描述了在四个总化学步骤中发明的布鲁顿酪氨酸激酶抑制剂 Branebrutinib (Bms-986195) 的商业途径.高通量实验 (Hte) 的执行与所提出的合成路线中的第一性原理方法相结合,能够识别一种新的吲哚化反应,该反应迅速产生高合成复杂性,作为合成的核心.路线设计期间的并行 Hte 策略能够在短时间内对多个选项进行有效和快速的评估,以完成严格的工艺开发,同时降低与实施具有积极断开策略的新化学物质相关的风险.
Doi:10.1021/acs.Oprd.1C00443

专利信息

专利号:US-3959322-A
优先权日:1960-09-22
标 题:Synthesis of 13-alkyl-gon-4-ones
发明人：HUGHES GORDON ALAN; SMITH HERCHEL
权利人:SMITH HERCHEL
摘要:The preparation of 13-methylgon-4-enes and novel 13-polycarbonalkylgon-4-enes by a new total synthesis is described. 13-Alkylgon-4-enes having progestational, anabolic and androgenic activities are prepared by forming a tetracylic gonane structure unsaturated in the 1,3,5(10),9(11) and 14-positions, selectively reducing in the B- and C-rings, and converting the aromatic A-ring compounds so-produced to gon-4-enes by Birch reduction and hydrolysis.

专利号:US-8188113-B2
优先权日:2006-09-14
标 题 :Dihydropyridopyrimidinyl, dihydronaphthyidinyl and related compounds useful as kinase inhibitors for the treatment of proliferative diseases
发明人：FLYNN DANIEL L; PETILLO PETER A; KAUFMAN MICHAEL D; PATT WILLIAM C
权利人:FLYNN DANIEL L; PETILLO PETER A; KAUFMAN MICHAEL D; PATT WILLIAM C; DECIPHERA PHARMACEUTICALS INC
摘要:The present invention relates to novel dihydropyridopyrimidinyl, dihydronaphthyridinyl, and related compounds which are kinase inhibitors and modulator useful for the treatment of various diseases. More particularly, the invention is concerned with such compounds, kinase/compound adducts, methods of treating diseases, and methods of synthesis of the compounds. Preferably, the compounds are useful for the modulation of kinase activity of Raf kinases and disease polymorphs thereof. Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant melanoma, colorectal cancer, ovarian cancer, papillary thyroid carcinoma, non small cell lung cancer, and mesothelioma. Compounds of the present invention also find utility in the treatment of rheumatoid arthritis and retinopathies including diabetic retinal neuropathy and macular degeneration.

专利号:US-5656634-A
优先权日:1991-03-21
标题 :N-aryl and N-heteroarylamide and urea derivatives as inhibitors of acyl coenzyme A: cholesterol acyl transferase (ACAT)
发明人：CHANG GEORGE; HAMANAKA ERNEST S; MCCARTHY PETER A; TRUONG THIEN V; WALKER FREDERICK J
权利人:PFIZER
摘要:Compounds of the formula ##STR1## the pharmaceutically acceptable salts thereof, wherein Q and R 1 are as defined below, and novel carboxylic acid and acid halide intermediates used in the synthesis of such compounds. The compounds of formula I are inhibitors of acyl coenzyme A: cholesterol acyltransferase (ACAT) and are useful as hypolipidemic and antiatherosclerosis agents.

专利号:US-6005103-A
优先权日:1993-11-19
标题 :Pyrone derivatives as protease inhibitors and antiviral agents
发明人：DOMAGALA JOHN MICHAEL; LUNNEY ELIZABETH; PARA KIMBERLY SUZANNE; PRASAD JOSYULA VENKATA NAGENDR; TAIT BRADLEY DEAN
权利人:WARNER LAMBERT CO
摘要:The present invention relates to novel tri- and tetrasubstituted pyrones and related structures which potently inhibit the HIV aspartyl protease blocking HIV infectivity. The pyrone derivatives are useful in the development of therapies for the treatment of bacterial and viral infections and diseases, including AIDS. The present invention is also directed to methods of synthesis of multifunctionalized pyrones and of related structures.

专利号:US-11434242-B2
优先权日:2017-12-04
标题:Dopamine-b-hydroxylase inhibitors
发明人：KISS LASZLO ERNO; BELIAEV ALEXANDER; ROSSI TINO; PALMA PEDRO NUNO LEAL; SOARES DA SILVA PATRÃ?CIO MANUEL VIEIRA ARAUJO; PINTO RUI; CARDONA FRANCISCO
权利人:BIAL PORTELA & Cª S A; BIAL—PORTELA & CA S A
摘要:This invention relates to: (a) compounds of formula Ia (with R1, R4 to R6, n and A as defined herein) and pharmaceutically acceptable salts or solvates thereof that are useful as dopamine-β-hydroxylase inhibitors; (b) pharmaceutical compositions (comprising such compounds, salts or solvates; (c) the use of such compounds, salts or solvates in therapy; (d) therapeutic methods of treatment using such compounds, salts or solvates; and (e) processes and intermediates useful for the synthesis of such compounds.

专利号:EP-1836163-B1
优先权日:2004-12-23
标题 :Pyrrolidine derivatives for the treatment of a disease depending on the activity of renin
发明人：BREITENSTEIN WERNER; COTTENS SYLVAIN; EHRHARDT CLAUS; JACOBY EDGAR; LORTHIOIS EDWIGE LILIANE JEANNE; MAIBAUM JUERGEN KLAUS; OSTERMANN NILS; SELLNER HOLGER; SIMIC OLIVER
权利人:NOVARTIS AG
摘要:Novel 3-mono-, 3,4-di- and 3,4,4,-tri-substituted pyrrolidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on inappropriate activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on inappropriate activity of renin; the use of a compound of that class in the treatment of a disease that depends on inappropriate activity of renin; pharmaceutical formulations comprising a said substituted pyrrolidine compound, and/or a method of treatment comprising administering a said substituted pyrrolidine compound, a method for the manufacture of said substituted pyrrolidine compounds, and novel intermediates and partial steps for their synthesis are described. The substituted pyrrolidine compounds are especially of the formula I wherein the substituents are as described in the specification.