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    PHARMACEUTICALLY ACTIVE DIMERS LINKED THROUGH PHENOLIC HYDROXYL GROUPS
    1.
    发明申请
    PHARMACEUTICALLY ACTIVE DIMERS LINKED THROUGH PHENOLIC HYDROXYL GROUPS 审中-公开

    公开(公告)号：US20160368931A1

    公开(公告)日：2016-12-22

    申请号：US15074933

    申请日：2016-03-18

    申请人： OrphoMed, Inc.

    发明人： Nikhilesh Nihala Singh

    IPC分类号： C07D519/00 ,  C07C217/70 ,  C07C217/74

    摘要： Pharmaceutically active homo-dimers of opioid and other pharmaceutically active agents characterized by a single phenolic hydroxyl group wherein the respective monomers are ether-linked through such groups by an ethylene residue. The dimers share the receptor pharmacology of the corresponding monomer, in particular cases are non-absorbed, and the ether link of the dimers is particularly resistant to metabolism when administered to a subject, all conferring divers advantages relative to the corresponding monomers. Exemplary of the dimers are those of buprenorphine, naloxone, naltrexone, des-venlafaxine, albuterol and acetaminophen.

    Process for the synthesis of arformoterol
    3.
    发明授权
    Process for the synthesis of arformoterol 有权
    合成阿霉素的方法

    公开(公告)号：US09029421B2

    公开(公告)日：2015-05-12

    申请号：US12995016

    申请日：2009-06-02

    申请人： Vaishali Vaman Haldavanekar ,  Mangesh Prabhu ,  Dharmaraj Ramachandra Rao ,  Rajendra Narayanrao Kankan

    发明人： Vaishali Vaman Haldavanekar ,  Mangesh Prabhu ,  Dharmaraj Ramachandra Rao ,  Rajendra Narayanrao Kankan

    IPC分类号： C07C217/86 ,  C07C213/02 ,  C07C217/70 ,  C07C213/00 ,  C07C213/08 ,  C07C213/10 ,  C07C231/02 ,  C07C233/43

    CPC分类号： C07C231/10 ,  C07B2200/07 ,  C07C213/00 ,  C07C213/08 ,  C07C213/10 ,  C07C217/60 ,  C07C217/86 ,  C07C231/02 ,  C07C233/43

    摘要： The present invention provides a process for preparing a compound of formula (VI) or a salt thereof, the process comprising: (i) reacting 4-methoxyphenyl acetone with an amine of formula (VIII) under conditions of reductive amination to produce a compound of formula (II) or a salt thereof, wherein there is no isolation of an imine intermediate formed during the reductive amination; (ii) condensing the compound (II) or the acid addition salt thereof with an α-haloketone of formula (III) to produce the compound of formula (IV); (iii) reducing the compound (IV) to a compound of formula (V); and (iv) reducing the compound (V) to the compound of formula (VI), wherein the reduction is carried out in the presence of either (1) a hydrogen donating compound in the presence of a hydrogen transfer catalyst; or (2) ammonium formate using a hydrogenation catalyst, wherein R1 and R2 are independently optionally substituted arylalkyl, and Hal is selected from chloro or bromo.

    摘要翻译： 本发明提供了制备式（Ⅵ）化合物或其盐的方法，该方法包括：（ⅰ）在还原胺化的条件下使4-甲氧基苯基丙酮与式（Ⅷ）的胺反应，得到 式（II）或其盐，其中在还原胺化期间不形成亚胺中间体的分离; （ii）将化合物（II）或其酸加成盐与式（III）的α-卤代酮缩合以制备式（IV）化合物; （iii）将化合物（IV）还原成式（V）的化合物; 和（iv）将化合物（V）还原成式（VI）化合物，其中还原反应在（1）给氢化合物存在下，在氢转移催化剂存在下进行; 或（2）使用氢化催化剂的甲酸铵，其中R 1和R 2独立地是任选取代的芳烷基，Hal选自氯或溴。

    Optically active fluorinated vasoconstrictors, methods for making them, and anesthetic formulations comprising them
    4.
    发明授权
    Optically active fluorinated vasoconstrictors, methods for making them, and anesthetic formulations comprising them 失效
    光学活性氟化血管​​收缩剂，其制备方法和包含它们的麻醉剂制剂

    公开(公告)号：US06900203B2

    公开(公告)日：2005-05-31

    申请号：US10190856

    申请日：2002-07-08

    申请人： Hamilton J. Lenox ,  Elena Terentieva ,  Mikhail Y. Gololobov

    发明人： Hamilton J. Lenox ,  Elena Terentieva ,  Mikhail Y. Gololobov

    IPC分类号： A61K31/137 ,  A61K31/167 ,  C07C215/60 ,  C07C217/70 ,  C07C233/18 ,  C07C255/37 ,  C12P13/00 ,  A61K31/535 ,  A61K31/135 ,  A61K31/16 ,  A61K31/24 ,  A61K31/445

    CPC分类号： C12P13/004 ,  A61K31/137 ,  A61K31/167 ,  C07B2200/07 ,  C07C215/60 ,  C07C217/70 ,  C07C233/18 ,  C07C255/37 ,  A61K2300/00

    摘要： (R)-6F-phenylephrine, essentially free of (S)-6F-phenylephrine, and an anesthetic formulation comprising (R)-6F-epinephrin or (R)-6F-phenylephrine and having improved stability compared to formulations containing their non-fluorinated analog, are disclosed. Further disclosed is a method of providing vasoconstriction in a mammal by administering the anesthetic formulation. The anesthetic composition can include an anesthetic, an (R)-chiral compound having the structure: wherein R1, R2, and R4 are independently selected from —H or —F, at least one of R1, R2, and R4 is —F, and R3 is selected from —OH, —H or —F, or a pharmaceutically acceptable salt or ester thereof, said vasoconstrictor being essentially free of the (S)-chiral form. Also, a method of chiral addition of cyanide to a ring-fluorinated phenaldehyde, employing an almond hydroxynitrile lyase enzyme, provided in the form of a reversibly soluble polymer conjugate ((R)-Finezyme™-H series biocatalysts) is disclosed. Several such biocatalysts are disclosed.

    摘要翻译： （R）-6F-去氧肾上腺素，以及包含（R）-6F-肾上腺素或（R）-6F-去氧肾上腺素）的麻醉剂制剂，并且与含有它们的非 - 氟化类似物。 进一步公开的是通过施用麻醉剂制剂在哺乳动物中提供血管收缩的方法。 麻醉剂组合物可以包括麻醉剂，具有以下结构的（R） - 手性化合物：其中R 1，R 2和R 4， 独立地选自-H或-F，R 1，R 2和R 4中的至少一个是-F，R 选自-OH，-H或-F，或其药学上可接受的盐或酯，所述血管收缩剂基本上不含（S） - 手性形式。 此外，公开了以可逆可溶性聚合物缀合物（（R）-Finezyme TM -H系列生物催化剂）的形式提供的使用杏仁羟基腈裂解酶的氰化氰手性加入到环氟化苯醛中的方法。 公开了几种这样的生物催化剂。