CAS: 34580-13-7; 4-(1-Methylpiperidin-4-Ylidene)-4H-Benzo[4,5]Cyclohepta[1,2-B]Thiophen-10(9H)-One

该化合物是一种主要用作抗口炎和甲状腺细胞稳定剂的药物化合物,通常用于治疗哮喘和抗过敏性鼻炎等过敏条件,被归类为二苯环戊戊基苯衍生物,并展示了一种双重行动机制:它会对抗甲胺H1受体,并抑制胸腔内发炎器的释放;Ketototifen通常以其发泡盐形式施用,这可增强它的溶性,并增加生物利用率;该物质的特点是水溶性相对较低,但有机溶剂中可溶性较易溶.Ketotifen的半衰期中度,允许在临床环境中每天服一至两次药,副作用可能包括镇静剂,干口腔和胃肠紊乱,这在抗口炎中很常见.其安全情况是通过广泛的临床使用而确定的,它是一种长期性过敏性治疗的可选用方法.与任何专业的药物一样,它使用基托伊夫医疗指导之下必须使用.

结构式图片

欧盟法规

ECHA物质C&L通报REACH预注册

上下游产品

CAS号59743-88-3 10-甲氧基-4-(1-甲基-... | CAS号126939-27-3 10-hydroxy-10-(... | CAS号59743-84-9 10-甲氧基-4H-苯并[4,... | CAS号5570-77-4 1-甲基-4-氯哌啶 | CAS号34580-12-6 4-(10-bromo-ben... | CAS号1622-55-5 9, 10-二氢-4H-苯并[... | CAS号34580-10-4 9,10-DIBROMO-9,... | CAS号63463-36-5 magnesium,1-met... | CAS号34580-11-5 10-bromo-4H-ben... | CAS号88456-70-6 10-(1-methyl-1-... | CAS号43076-12-6 10-(1-methylpip... | CAS号43076-16-0 9,10-二氧代酮替芬

合成工艺路线路线简述

  • 合成目标产物 Ketotifen 主要起始原料 Benzo[b]Thiophen-10-Methoxycycloheptanone
  • (文献来源)合成步骤主要原料 Benzo[b]Thiophen-10-Methoxycycloheptanone
10-甲氧基-4-(1-甲基-4-哌啶基)-4H-苯并[4,5]环庚三烯并[1,2-B]噻吩-4-醇置于盐酸体系中,化学反应 1.0H,反应生成 酮替芬
参考文献:Untersuchungenüber合成arzneimittel 9-和10-Oxo-衍生物von 9,10-Dihydro-4 H-Benzo [4,5] Cyclohepta-[1,2-B]噻吩的合成药物.9,10-二氢-4 H-苯并-[4,5]-环庚[1,2 B]噻吩的9-和10-氧代衍生物
标题:Untersuchungenüber合成arzneimittel 9-和10-Oxo-衍生物von 9,10-Dihydro-4 H-Benzo [4,5] Cyclohepta-[1,2-B]噻吩的合成药物.9,10-二氢-4 H-苯并-[4,5]-环庚[1,2 B]噻吩的9-和10-氧代衍生物
摘要:Verschiedene Synthesen Zur Herstellung Von 9-Oxo-9,10-Dihydro-4 H-Benzo [4,5] Cyclohepta [1,2-B]噻吩17和10-Oxo-9,10-Dihydro-4 H-Benzo [4,5] Cyclohepta [1,2-B]噻吩18(25),在4-Stellung中的1-烷基-4-Piperidyliden-Gruppe分子,9,10-Dihydro-4 H-苯并[4,5]]环庚[1,2-B]噻吩-4-Onen 1 Bzw. 达芬(folgestufen Davon),韦登.贝希里本(werden Beschrieben).als Weitere导数信德死-N-氧化物26,模具9-Und 10-羟基-衍生物27 Und 28,模具9-Und 10肟29 Und 30Sowie Ein
DOI:10.1002/hlca.19760590316

海关参考信息

专利信息


专利号:US-8734846-B2
优先权日:2008-06-16
标 题 :Methods for the preparation of targeting agent functionalized diblock copolymers for use in fabrication of therapeutic targeted nanoparticles
发明人:ALI MIR M; HRKACH JEFF; ZALE STEPHEN E; ALVAREZ DE CIENFUEGOS LUIS
权利人:BIND BIOSCIENCES INC
摘要:This application provides nanoparticles and methods of making nanoparticles using pre-functionalized poly(ethylene glycol)(also referred to as PEG) as a macroinitiator for the synthesis of diblock copolymers. Ring opening polymerization yields the desired poly(ester)-poly (ethylene glycol)-targeting agent polymer that is used to impart targeting capability to therapeutic nanoparticles. This “polymerization fromâ€? approach typically employs precursors of the targeting agent wherein the reactivity of functional groups of the targeting agent is masked using protecting groups. Also described is a “coupling toâ€? that utilized the poly(ethylene glycol)-targeting agent conjugate where the targeting agent remains in its native un-protected form. This method uses “orthogonalâ€? chemistry that exhibit no cross reactivity towards functional groups typically found within targeting agents of interest.

专利号:US-7919505-B2
优先权日:2006-07-11
标题 :Xinafoate salt of a substituted 5-oxazol-2-yl-quinoline compound
发明人:TING PAULINE C; LEE JOE F; FENG KUNG-I; REEDER MICHAEL R; TRZASKA SCOTT T; ZHU MAN; MAO CHEN; FILIPOV DIMITAR L; ZARKADAS DIMITRIOS N
权利人:SCHERING CORP
摘要:The present invention relates to the compound of the formula n nTo methods of treating upper and lower obstructive airway diseases using said compound, to formulations comprising it, and to polymorphs and processes of synthesis of the polymorphic forms.

专利号:US-2011003780-A1
优先权日:2007-07-10
标题:Hydrogen chloride salt of a substituted 5-oxazol-2-yl-quinoline compound and a process for the production thereof
发明人:ZHU MAN
权利人:SCHERING CORP
摘要:The present invention relates to the compound of the Formula I: n n n n n n n n n n and to methods of treating upper and lower obstructive airway diseases using said compound, to formulations comprising it, and to a particular crystalline form and processes of synthesis of the crystalline form. n IM=105109

专利号:US-5922335-A
优先权日:1995-05-15
标 题:Uses for ascorbyl-phosphoryl-cholesterol in topical compositions
发明人:PTCHELINTSEV DMITRI
权利人:AVON PROD INC
摘要:Novel uses of 3'-(L-ascorbyl-2-o-phosphoryl)-cholesterol, 3'-(L-ascorbyl-3-o-phosphoryl)-cholesterol, structural or functional isomers thereof and salts thereof (referred to collectively as 'APC compounds') are disclosed. Such novel uses include a method of reducing epidermal synthesis of abnormal elastin, especially epidermal synthesis of abnormal elastin that results from exposure to UV radiation. Also disclosed is a novel method of stimulating keratinocyte formation of triglycerides. In addition, a novel method of achieving antioxidant activity, both in the skin and also in topical compositions, is disclosed.

专利号:US-4678784-A
优先权日:1984-04-11
标题 :Method for the treatment of LHRH diseases and conditions
发明人:HO CHIH Y
权利人:MCNEILAB INC
摘要:Fused tetracyclic benzodiazepines of the formula (I): (I) where R1 is a cyclic amine such as 1-piperazine and R2 is H or a substituent as defined herein are useful as LHRH antagonizing agents. Also, methods for their synthesis, intermediates used in such synthesis, methods for use as medicaments and pharmaceutical compositions are described.

专利号:US-11993606-B2
优先权日:2015-10-16
标题:Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-n-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
发明人:MOHAMED MOHAMED-ESLAM F; OTHMAN AHMED A; PANGAN AILEEN L; SONG IN-HO; KLÜNDER BEN; VOSS JEFFREY W; PADLEY ROBERT J; CAMP HEIDI S
权利人:ABBVIE INC
摘要:The present disclosure relates to processes for preparing (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide, solid state forms thereof, and corresponding pharmaceutical compositions, methods of treatment (including treatment of rheumatoid arthritis and various spondyloarthritic conditions, including types of axial spondyloarthritis (axSpA)), kits, methods of synthesis, and products-by-process. In various aspects, provided are methods for treating active non-radiographic axSpA (nr-axSpA) and methods for treating active ankylosing spondylitis (AS).
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主要参考文献


1: Schwarzer G, Bassler D, Mitra A, Ducharme FM, Forster J. Ketotifen alone or as additional medication for long-term control of asthma and wheeze in children. Cochrane Database Syst Rev. 2004;(1):CD001384. Review. Review. Spanish. Review. Erratum in: Drugs 1991 Feb;41(2):192. Review. Review. German. Review. Review. French. Review. Polish. Review. Review. French. Review. Review. Hebrew. Review. Review.

合成参考文献


参考文献:10.1186/1475-2875-9-53
摘要:Sowunmi A, Adewoye EO, Gbotsho GO, Happi CT, Sijuade A, Folarin OA, Okuboyejo TM, Michael OS. Factors contributing to delay in parasite clearance in uncomplicated falciparum malaria in children. Malaria Journal. 2010 Feb 15;9(1):53. doi: 10.1186/1475-2875-9-53.
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