CAS: 499-67-2; Proparacaine Hydrochloride

该化合物是一种苯甲酸酯衍生物,具有氨基和丙氧功能组,为合成应用提供了多种可变性;二乙基乙基乙基能提高了有机溶剂的溶性,便利了药物和化学合成的使用;该化合物的双重功能 ----胺和酯组 ----使它成为设计药物候选物或精密化学品的宝贵中间体;丙氧组有助于亲脂性,有可能提高生物活性分子的膜渗透性;该化合物特别适合药用化学的改变,因为根据特定需要,物理化学特性至关重要;在标准条件下,高纯度和稳定性进一步确保研究和工业过程的可靠性能.

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CAS号736870-51-2 3-NITRO-4-PROPO... | CAS号616-82-0 3-硝基-4-羟基-苯甲酸 | CAS号35288-44-9 3-硝基-4-丙氧基苯甲酸

合成工艺路线路线简述

    📜3-硝基-4-丙氧基苯甲酸 2-(二乙胺基)乙酯置于铁粉,氯化铵体系中,用 乙醇,水 作为反应溶剂,化学反应生成 丙美卡因
    参考文献:Cn116178190
    标题:Cn116178190

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    专利信息


    专利号:US-5134146-A
    优先权日:1990-05-13
    标题:Substituted oxadiazoles and thiadiazoles for use in the treatment of glaucoma
    发明人:SHOWELL GRAHAM; LOTTI VICTOR
    权利人:MERCK SHARP & DOHME
    摘要:The use of compounds for formula (I): ##STR1## or a salt or prodrug thereof; wherein one of X, Y, or Z is an oxygen or sulphur atom and the other two are nitrogen atoms, and the dotted circle represents two double bonds thus forming a 1,3,4-oxadiazole, 1,2,4-oxadiazole, 1,3,4-thiadiazole or 1,2,4-thiadiazole nucleus; n R 1 represents a non-aromatic azacyclic or azabicyclic ring system selected from ##STR2## wherein the broken line represents an optional chemical bond; the substituents R 3 and R 4 may be present at any position, including the point of attachment to the oxa- or thia-diazole ring, and independently represent hydrogen, C 1-4 alkyl, halo, C 1-4 alkoxy, hydroxy or carboxy, or R 3 and R 4 together represent carbonyl; n the group R 5 represents hydrogen or C 1-4 alkyl; and n R 2 represents hydrogen, C 1-8 hydrogen, C 1-8 alkyl optionally substituted by hydroxy or fluoro, C 2-8 alkenyl, OR 7 , SR 7 , NR 7 R 8 , CN, CO 2 R 7 , CONR 7 R 8 OR NHCONHR 9 where R 9 is C 1-4 alkyl; wherein R 7 and R 8 independently represent hydrogen or saturated or unsaturated C 1-4 alkyl provided that, when R 7 and R 8 in NR 7 R 8 are both hydrogen, at least one of R 3 and R 4 is C 1-4 alkyl, n in the treatment of glaucoma, novel compounds having such use, formulations containing them and their synthesis.

    专利号:US-2002010128-A1
    优先权日:2000-04-13
    标题 :Treatment of hyperproliferative, inflammatory and related mucocutaneous disorders using inhibitors of mevalonate synthesis and metabolism
    发明人:PARKS THOMAS P; GRAYSON STEPHEN
    摘要:The present invention provides methods for treating a variety of hyperproliferative and inflammatory mucocutaneous disorders, including, basal cell carcinoma, squamous cell carcinoma, psoriasis and atopic dermatitis, as well as skin irritation and disorders associated with skin aging and skin photodamage using inhibitors of cholesterol metabolism. The present invention further relates to the discovery that the combined use of several inhibitors of cholesterol metabolism produces synergistic effects. Furthermore, the present invention is directed to the use of inhibitors of cholesterol metabolism as excipients to enhance the effects of antiinflammatory drugs.

    专利号:US-4975447-A
    优先权日:1983-02-04
    标 题:6-hydroxyethoxy-2-benzothiazolesulfonamide and topical treatment compositions and method for glaucoma
    发明人:SCHOENWALD RONALD D; BARFKNECHT CHARLES F
    权利人:UNIV IOWA RES FOUND
    摘要:A topical composition for eye treatment of glaucoma, comprising a small but pharmaceutically effective amount of an analog of benzothiazole-2-sulfonamide. The most preferred compound is 6-hydroxyethoxy-2-benzothiazolesulfonamide. The invention also relates to a method of topically treating glaucoma with eye drops to reduce intraocular pressure. Finally, disclosed is a method of synthesis of the preferred and highly effective benzothiazole-2-sulfonamide analogs, particularly the 6-hydroxyethoxy-2-benzothiazolesulfonamide compound.

    专利号:US-4975448-A
    优先权日:1983-02-04
    标题 :6-amino-2-benzothiazolesulfonamide and topical treatment compositions and method for glaucoma
    发明人:SCHOENWALD RONALD D; BARFKNECHT CHARLES F
    权利人:UNIV IOWA RES FOUND
    摘要:A topical composition for eye treatment of glaucoma, comprising a small but pharmaceutically effective amount of an analog of benzothiazole-2-sulfonamide. The most preferred compound is 6-amino-2-benzothiazolesulfonamide. The invention also relates to a method of topically treating glaucoma with eye drops to reduce intraocular pressure. Finally, disclosed is a method of synthesis of the preferred and highly effective benzothiazole-2-sulfonamide analogs, particularly the 6-amino-2-benzothiazolesulfonamide compound.

    专利号:US-6531614-B2
    优先权日:1993-12-15
    标题 :Method of prostaglandin synthesis
    发明人:CONROW RAYMOND E
    权利人:ALCON MFG LTD
    摘要:Methods of synthesizing 9-Halo-13,14-dihydroprostaglandins useful in the treatment of glaucoma and ocular hypertension are disclosed. Also disclosed are ophthalmic, pharmaceutical compositions comprising such prostaglandins.

    专利号:US-5512577-A
    优先权日:1994-06-02
    标 题:Bicyclic hexahydroaporphine and 1-benzyloctahydroisoquinoline therapeutic compositions and processes for utilizing said compositions
    发明人:ROCHE VICTORIA F; OHIA S EDET; ROCHE EDWARD B
    权利人:UNIV CREIGHTON
    摘要:The invention relates to the method of synthesis of bicyclic hexahydroaporphine compounds which may provide improved therapy for diseases characterized by an increase in intraocular pressure. More specifically, the present invention relates to the preparation of agents which may provide for improved treatment of patients with glaucoma or ocular hypertension. The present invention describes the intraocular pressure lowering capabilities of several of the bicyclic hexahydroaporphine structures.

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    主要参考文献


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    10: Gill FR, Murphy PJ, Purslow C. Topical anaesthetic use prior to rigid gas permeable contact lens fitting. Cont Lens Anterior Eye. 2017 Dec;40(6):424-431. doi: 10.1016/j.clae.2017.07.005. Epub 2017 Aug 12. doi: 10.1016/j.jaapos.2015.05.010. doi: 10.1111/vop.12440. Epub 2016 Dec 15. doi: 10.1097/ICO.0000000000001250.
    16: Zhang J, Yang M, Zhou M, He L, Chen N, Zakrzewska JM. Non-antiepileptic drugs for trigeminal neuralgia. Cochrane Database Syst Rev. 2013 Dec 3;(12):CD004029. doi: 10.1002/14651858.CD004029.pub4. Review. doi: 10.1016/j.jemermed.2015.06.069. Epub 2015 Aug 15. Review. doi: 10.1007/s10792-017-0587-2. Epub 2017 Jun 14. doi: 10.1186/s12917-018-1593-y. Erratum in: BMC Vet Res. 2018 Oct 8;14(1):305.

    合成参考文献


    摘要:Ma J, Kabiel M, Tucker BA, Ge J, Young MJ. Combining chondroitinase ABC and growth factors promotes the integration of murine retinal progenitor cells transplanted into Rho(-/-) mice. Mol Vis. 2011;17():1759–70.
    参考文献:10.2147/opth.s21247
    摘要:Almubrad TM, Osuagwu UL, Alabbadi I, Ogbuehi KC. Comparison of the precision of the Topcon SP-3000P specular microscope and an ultrasound pachymeter. Clin Ophthalmol. 2011;5():871–6.
    参考文献:10.1007/s10792-011-9458-4
    摘要:Bhartiya S, Bali SJ, Sharma R, Chaturvedi N, Dada T. Comparative evaluation of TonoPen AVIA, Goldmann applanation tonometry and non-contact tonometry. Int Ophthalmol. 2011 Aug;31(4):297–302. doi: 10.1007/s10792-011-9458-4.
    参考文献:10.1155/2011/769571
    摘要:Espiritu CRG, Sy MEA, Tayengco TLG. Efficacy and Tolerability of a Combined Moxifloxacin/Dexamethasone Formulation for Topical Prophylaxis in Phacoemulsification: An Open-Label Single-Arm Clinical Trial. Journal of Ophthalmology. 2011;2011():1–5. doi: 10.1155/2011/769571.
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