CAS: 92206-54-7; 6-(Propyl(2-(Thiophen-2-yl)Ethyl)Amino)-5,6,7,8-Tetrahydronaphthalen-1-Ol

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CAS号40412-06-4 2-(噻吩-2-基)乙基 4-... | CAS号78950-82-0 5,6,7,8-四氢-6-(丙... | CAS号1918-77-0 2-噻吩乙酸 | CAS号32940-15-1 5-甲氧基-2-萘满酮 | CAS号78598-91-1 2-丙氨基-5-甲氧基四嗪 | CAS号101945-65-7 (S)-5-甲氧基-n-丙基-...

📜5-甲氧基-2-萘满酮置于硼烷-三甲胺络合物,氢溴酸,Sodium Cyanoborohydride,溶剂黄146体系中,用 甲醇,Xylene 作为反应溶剂,化学反应生成 罗替戈汀
参考文献:对2-氨基四氢萘的多巴胺d2,D3和d4受体的亲和力.d2激动剂结合与确定受体亚型选择性的相关性.
标题:对2-氨基四氢萘的多巴胺d2,D3和d4受体的亲和力.d2激动剂结合与确定受体亚型选择性的相关性.
摘要:制备了一系列2-氨基四氢化萘,在5-或7位上被甲氧基或羟基取代,并具有不同的n-烷基或n-芳基烷基取代基,并在人多巴胺(da)d2的结合测定中进行了评估,D3和d4受体.该系列的某些成员是在以前的研究中准备的,但从未在体外用单受体亚型进行测试,因此再次进行了检查.所测试的2-氨基四氢化萘均未显示出对多巴胺d4受体的高亲和力.但是,如化合物11-15和21-26所示,许多2-氨基四氢萘林对d2和d3 Da受体均显示出高亲和力,而有些对da D3受体具有合理的选择性.2-氨基四氢萘林对d21受体的亲和力取决于所用放射性配体(激动剂或拮抗剂)的类型.激动剂亲和力数据,
DOI:10.1021/jm960345L

专利信息

专利号:US-2024082118-A1
优先权日:2021-05-19
标 题:Topical compositions and methods of preparing the same
发明人：ABRAMOVICH SAGI; AVIDOR GAL; LANDA BENZION
权利人:LANDA LABS 2012 LTD
摘要:There is disclosed a composition comprising a water-insoluble thermoplastic compound capable of stimulating collagen synthesis (CSSC), the CSSC having a molecular weight of more than 0.6 kDa and being dispersed in a polar carrier as nano-elements having an average diameter of 200 nm or less and a viscosity of 107 mPa·s or less. The nano-elements of CSSC can be capable of stimulating the synthesis of skin proteins and/or enabling the delivery of active agents upon their application to a surface to be treated therewith. Methods for preparing the compositions and uses thereof are also provided.

专利号:US-8729306-B2
优先权日:2010-02-05
标 题:Process for the preparation of nitrogen substituted aminotetralins derivatives
发明人：VASSELIN DAVID; CARLY NICOLAS; ATES CELAL
权利人:VASSELIN DAVID; CARLY NICOLAS; ATES CELAL; UCB PHARMA GMBH
摘要:The present invention provides an alternative synthesis of N-substituted aminotetralines which synthesis comprises catalytic asymmetric hydrogenation of compounds of general formula (A).

专利号:US-11766432-B2
优先权日:2018-07-27
标题 :Cleavable conjugates of catechol compounds and water-soluble polymers and methods of treatment using the same
发明人：BENTLEY MICHAEL; FANG ZHIHAO; WEIMER REBECCA; VIEGAS TACEY; MOREADITH RANDALL
权利人:SERINA THERAPEUTICS INC
摘要:Described are conjugates comprising a water-soluble polymer linked to a compound comprising a catechol moiety via a cleavable linkage, wherein the cleavable linkage is formed between the water-soluble polymer and a first phenolic hydroxyl group of the catechol moiety and a second phenolic hydroxyl group of the catechol moiety is linked to a blocking group wherein the rate of hydrolytic release of the compound comprising the catechol moiety is controlled, at least in part, through structure or design of the blocking group on the second phenolic hydroxyl group of the catechol moiety. Therefore, the rate of hydrolytic release of the compound comprising the catechol moiety can be tuned through structural design of the group on the second phenolic hydroxyl group of the catechol moiety. Compounds used in the synthesis of the described conjugates and methods of using the described conjugate and other compounds in the treatment of dopamine-responsive disorders are also described.

专利号:US-8981121-B2
优先权日:2010-06-25
标 题 :Process for the preparation of nitrogen substituted aminotetralins derivatives
发明人：ATES CELAL; SCHULE ARNAUD; PALACIO MAGALI; DEUTSCH PAUL; VASSELIN DAVID; CARLY NICOLAS; PHADTARE GANESH; YERANDE SWAPNIL; DELATINNE JEAN-PIERRE; ESCUDERO HERNANDEZ MARIA LUISA; PINILLA VERONIQUE
权利人:ATES CELAL; SCHULE ARNAUD; PALACIO MAGALI; DEUTSCH PAUL; VASSELIN DAVID; CARLY NICOLAS; PHADTARE GANESH; YERANDE SWAPNIL; DELATINNE JEAN-PIERRE; ESCUDERO HERNANDEZ MARIA LUISA; PINILLA VERONIQUE; UCB PHARMA GMBH
摘要:The present invention provides an alternative synthesis of N-substituted aminotetralines comprising resolution of N-substituted aminotetralins of formula (II), wherein R 1 , R 2 and R 3 are as defined for compound of formula (I).

专利号:US-10022366-B2
优先权日:2013-04-23
标 题:Extending and maintaining micropore viability of microneedle treated skin with lipid biosynthesis inhibitors for sustained drug delivery
发明人：STINCHCOMB AUDRA L; GHOSH PRIYANKA
权利人:STINCHCOMB AUDRA L; GHOSH PRIYANKA; UNIV MARYLAND; UNIV KENTUCKY RES FOUND
摘要:Microneedles and their use as a physical skin permeation enhancement technique facilitate drug delivery across the skin in therapeutically relevant concentrations. Micropores created in the skin by MNs reseal because of normal healing processes of the skin, thus limiting the duration of the drug delivery window. Pore lifetime enhancement strategies can increase effectiveness of MNs as a drug delivery mechanism by prolonging the delivery window. Fluvastatin (FLU) was used to enhance pore lifetime by inhibiting the synthesis of cholesterol, a major component of the stratum corneum lipids. The skin recovered within a 30-45-min time period following the removal of occlusion, and there was no significant irritation observed due to the treatment compared to the control sites. Thus, it can be concluded that localized skin treatment with FLU can be used to extend micropore lifetime and deliver drugs for up to 7 days across MN-treated skin.

专利号:WO-2025128098-A1
优先权日:2023-12-13
标 题 :Solid oral dosage forms, kits, and methods of using the same
发明人：LI YING; LANGER ROBERT; TRAVERSO CARLO
权利人:MASSACHUSETTS INST TECHNOLOGY; BRIGHAM & WOMENS HOSPITAL INC
摘要:Provided herein are solid oral dosage forms, methods, and kits useful, e.g, for the extension of the residence time of active pharmaceutical agents in vivo by the synthesis of a polymer in situ in a subject. In particular, the solid oral dosage forms, methods, and kits disclosed herein are particularly useful for drugs that require more than once daily administration (e.g, drugs that have short half-lives).