CAS: 81801-12-9; Xamoterol

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CAS号76167-36-7 N-[[N-benzyl[3-... | CAS号69630-05-3 N-[2-[N-benzyl[...

📜Phenyl N-<2-<3-<4-(Benzyloxy)Phenoxy>-2-Hydroxypropyl>Amino>Ethyl>Carbamate置于palladium On Activated Charcoal 氢气,溶剂黄146体系中,用 甲苯 作为反应溶剂,化学反应 19.5H,反应生成 扎莫特罗
参考文献:.Beta.-Adrenoceptor Stimulant Properties Of Amidoalkylamino-Substituted 1-Aryl-2-Ethanols And 1-(Aryloxy)-2-Propanols
标题:.Beta.-Adrenoceptor Stimulant Properties Of Amidoalkylamino-Substituted 1-Aryl-2-Ethanols And 1-(Aryloxy)-2-Propanols
摘要:Parallel Series Of 2-[(2-Amidoethyl)Amino]-1-Arylethanols And 1-[(2-Amidoethyl)Amino]-3-(Aryloxy)-2-Propanols Have Been Prepared,And The Compounds Were Tested As Beta-Adrenoceptor Stimulants On The Heart And Circulation Of The Dog. The Corresponding 2-(Alkylamino)-1-Arylethanols And 3-(Alkylamino)-2-Propanols Have Been Tested For Comparison And The Structure-Activity Relationships (Sar) Examined. The Arylethanols Are Potent Full Agonists,Showing Selectivity For The Heart Relative To Blood Vessels,While The (Aryloxy)Propanols Are Even More Cardioselective And Are Partial Agonists. Within A Narrow Series Of 1-[(Amidoethyl)Amino]-3-(4-Hydroxyphenoxy)-2-Propanols,Careful Examination Of The Sar Of The Amide Group Showed That Great Variation In Cardioselectivity And Degree Of Agonism May Be Produce. From This Study Ici 118587,N-[20[[2-Hydroxy-3-(4-Hydroxyphenoxy)Propyl]Amino]Ethyl]-4-Morpholinecarboxamide,Was Selected For Its High Cardioselectivity And 50% Agonist Properties. This Compound In Under Clinical Evaluation As A Cardiac Stimulant.
DOI:10.1021/jm00135A015

专利信息

专利号:US-6683189-B1
优先权日:1996-02-26
标 题 :Method for the synthesis of pyrrole and imidazole carboxamides on a solid support
发明人：DERVAN PETER B; BAIRD ELDON
权利人:CALIFORNIA INST OF TECHN
摘要:The present invention describes a novel method for the solid phase synthesis of polyamides containing imidazole and pyrrole carboxamides. The polyamides are prepared on a solid support from aromatic carboxylic acids and aromatic amines with high stepwise coupling yields (>99%), providing milligram quantities of highly pure polyamides. The present invention also describes the synthesis of analogs of the natural products Netropsin and Distamycin A, two antiviral antibiotics. The present invention also describes a novel method for the solid phase synthesis of imidazole and pyrrole carboxamide polyamide-oligonucleotide conjugates. This methodology will greatly increase both the complexity and quantity of minor-groove binding polyamides and minor-groove binding polyamide-oligonucleotide conjugates which can be synthesized and tested.

专利号:US-9353057-B2
优先权日:2003-12-30
标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof
发明人：GALLOP MARK A; DAI XUEDONG; SCHEUERMAN RANDALL A; RAILLARD STEPHEN P; MANTHATI SURESH K; YAO FENMEI; PHAN THU; LUDWIKOW MARIA; PENG GE; BHAT SEEMA
权利人:XENOPORT INC
摘要:Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.

专利号:US-10925977-B2
优先权日:2006-10-05
标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications
发明人：YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S
权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS
摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.

专利号:US-2008287407-A1
优先权日:2003-12-10
标题 :Nitric Oxide Releasing Pyruvate Compounds, Compositions and Methods of Use
发明人：GARVEY DAVID S; FANG XINQIN; KHANAPURE SUBHASH P; RANATUNGA RAMANI R; WEY SHIOW-JYI
权利人:NITROMED INC
摘要:The invention describes novel nitrosated and/or nitrosylated pyruvate compounds and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated and/or nitrosylated pyruvate compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one pyruvate compound and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one pyruvate compound, that is optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating diseases resulting from oxidative stress, diabetes, reperfusion injury following ischemia, preservation of tissues, organs, organ parts and/or limbs.

专利号:US-8771639-B2
优先权日:2007-01-05
标 题 :Methods for preparing composites of substrate-molecular sieve
发明人：YOON KYUNG BYUNG; LEE JIN SEOK; KIM JAE HYUN; LEE YOUNG JU; JEONG NAK CHEON
权利人:YOON KYUNG BYUNG; LEE JIN SEOK; KIM JAE HYUN; LEE YOUNG JU; JEONG NAK CHEON; UNIV SOGANG IND UNIV COOP FOUN
摘要:The present invention relates to a method for preparing composites of substrate-molecular sieve, in particular, to a method for preparing a composite of substrate-molecular sieve, which comprises applying a physical pressure to molecular sieve crystals against a substrate to form a chemical bond between the molecular sieve crystal and the substrate. The present invention requiring no solvents, reactors and other equipments enables molecular sieve crystals to be stably attached to the surface of substrates through various chemical bonds, particularly ionic present invention ensures the synthesis of substrate-molecular sieve composites with enhanced attachment rate, degree of lateral close packing (DCP) and attachment strength in more time-saving and energy-saving manners. The present method works well for molecular sieve crystals with lager sizes (e.g., more than 3 μm) with no generation of parasitic crystals. Furthermore, the present invention shows excellent applicability to large substrates, enabling the mass production of substrate-molecular sieve composites.

专利号:US-8604213-B2
优先权日:2008-10-21
标 题 :Fluorination of aromatic ring systems
发明人：DIMAGNO STEPHEN
权利人:DIMAGNO STEPHEN; NUTECH VENTURES
摘要:This disclosure relates to reagents and methods useful in the synthesis of aryl fluorides, for example, in the preparation of 18 F labeled radiotracers. The reagents and methods provided herein may be used to access a broad range of compounds, including aromatic compounds, heteroaromatic compounds, amino acids, nucleotides, and synthetic compounds.