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    Par-2-activating peptide derivative and pharmaceutical composition using the same
    1.
    发明授权
    Par-2-activating peptide derivative and pharmaceutical composition using the same 失效
    对二激活肽衍生物和使用其的药物组合物

    公开(公告)号：US07541339B2

    公开(公告)日：2009-06-02

    申请号：US10517803

    申请日：2003-06-10

    申请人： Robert Ramage ,  Robin Plevin ,  Kevin Thomas Shaw ,  Lu Jiang ,  Louise Claire Young ,  Alan Lang Harvey ,  Pu Wang ,  Toru Kanke ,  Junichi Kawagoe ,  Mototsugu Kabeya

    发明人： Robert Ramage ,  Robin Plevin ,  Kevin Thomas Shaw ,  Lu Jiang ,  Louise Claire Young ,  Alan Lang Harvey ,  Pu Wang ,  Toru Kanke ,  Junichi Kawagoe ,  Mototsugu Kabeya

    IPC分类号： A61K38/08 ,  C07K7/06

    CPC分类号： C07K14/705 ,  A61K38/00 ,  C07K7/06

    摘要： The present invention relates to a peptide derivative represented by the general formula (I) or a salt thereof: Z-(CH2)n—CO—NH-Leu-Ile-Gly-AA1-AA2-CO—R (I) wherein Z represents an aryl group which may or may not have a substituent or a heteroaryl group which may or may not have a substituent; n represents 0, 1 or 2: AA1-AA2 represents Lys-Val or Arg-Leu; and R represents —OH or —NH2, and relates to a pharmaceutical composition comprising a peptide derivative represented by the general formula (I) or a salt thereof, and a pharmaceutically acceptable carrier thereof. The peptide derivative is useful as a prophylactic and therapeutic agent of dysfunction of masticatory, dysphagia, dysgeusia, ozostomia, intra-oral cavity dysphoria, intra-oral cavity infections, intra-oral cavity inflammations, dry eye, ectocornea detachment, keratitis, corneal ulcer, conjunctivitis, stomach ulcer, duodenal ulcer, gastritis, diarrhea, enteritis or Sjogren's syndrome.

    摘要翻译： 本发明涉及由通式（I）表示的肽衍生物或其盐：Z-（CH2）n-CO-NH-Leu-Ile-Gly-AA1-AA2-CO-R（Ⅰ）其中Z 表示可以具有也可以不具有取代基的芳基或可以具有取代基的杂芳基; n表示0,1或2：AA1-AA2表示Lys-Val或Arg-Leu; 和R表示-OH或-NH 2，并且涉及包含由通式（I）表示的肽衍生物或其盐及其药学上可接受的载体的药物组合物。 肽衍生物可用作咀嚼，吞咽困难，发重症，口臭，口腔内烦躁，口腔内感染，口腔内炎症，干眼症，异位角脱落，角膜炎，角膜溃疡功能障碍的预防和治疗剂 ，结膜炎，胃溃疡，十二指肠溃疡，胃炎，腹泻，肠炎或干燥综合征。

    Support for synthesis and purification of compounds
    3.
    发明授权
    Support for synthesis and purification of compounds 失效
    支持化合物的合成和纯化

    公开(公告)号：US06566520B2

    公开(公告)日：2003-05-20

    申请号：US09291524

    申请日：1999-04-14

    申请人： Sheila Helen DeWitt ,  Robert Ramage ,  Alasdair Arthur MacDonald

    发明人： Sheila Helen DeWitt ,  Robert Ramage ,  Alasdair Arthur MacDonald

    IPC分类号： C07D40100

    CPC分类号： C12N15/8297 ,  C07C69/00 ,  C07C2603/00 ,  C07D215/56

    摘要： A method for the preparation and purification of compounds using a novel support, a tetrabenzo [a, c, g, i]-fluorene group (Tbf) comprising reacting a building block (A) containing a Tbf group (Tbf-A), with a second building block (B), to afford an intermediate compound (Tbg-A-B) followed by purifying the intermediate compound by adsorption on a carbon support, removing the intermediate compound from the support with a solvent and repeating the previous reactions using the required number of building blocks to synthesize the compounds followed by removal of the Tbf group to afford the desired compounds.

    摘要翻译： 使用新型载体四丁苯并[a，c，g，i] - 芴基（Tbf）制备和纯化化合物的方法，包括使含有Tbf基团（Tbf-A）的结构单元（A）与 第二构建块（B），得到中间体化合物（Tbg-AB），然后通过在碳载体上吸附纯化中间体化合物，用溶剂从载体中除去中间体化合物，并使用所需数量重复以前的反应 的组合物合成化合物，然后除去Tbf基团，得到所需化合物。

    Support for synthesis and purification of compounds
    4.
    发明授权
    Support for synthesis and purification of compounds 失效
    支持化合物的合成和纯化

    公开(公告)号：US5977400A

    公开(公告)日：1999-11-02

    申请号：US48166

    申请日：1998-03-25

    申请人： Sheila Helen DeWitt ,  Robert Ramage ,  Alasdair Arthur MacDonald

    发明人： Sheila Helen DeWitt ,  Robert Ramage ,  Alasdair Arthur MacDonald

    IPC分类号： C07C69/00 ,  C07D215/56 ,  C12N15/82 ,  C07C69/76 ,  C07D215/16 ,  C07D401/00

    CPC分类号： C12N15/8297 ,  C07C69/00 ,  C07D215/56 ,  C07C2103/00

    摘要： A method for the preparation and purification of compounds using a novel support, a tetrabenzo[a,c,g,i]fluorene group (Tbf) comprising reacting a building block (A) containing a Tbf group (Tbf-A), with a second building block (B), to afford an intermediate compound (Tbg-A-B) followed by purifying the intermediate compound by adsorption on a carbon support, removing the intermediate compound from the support with a solvent and repeating the previous reactions using the required number of building blocks to synthesize the compounds followed by removal of the Tbf group to afford the desired compounds.

    摘要翻译： 一种使用新型载体，四苯并[a，c，g，i]芴基（Tbf）制备和纯化化合物的方法，包括使含有Tbf基团（Tbf-A）的结构单元（A）与 第二组合物（B），得到中间体化合物（Tbg-AB），然后通过在碳载体上吸附纯化中间体化合物，用溶剂从载体中除去中间体化合物，并使用所需数量的 合成化合物，然后除去Tbf基团，得到所需化合物。

    Purification means
    5.
    发明申请
    Purification means 审中-公开
    净化手段

    公开(公告)号：US20070010673A1

    公开(公告)日：2007-01-11

    申请号：US10558870

    申请日：2004-06-01

    申请人： Alastair Hay ,  Graham Cotton ,  Robert Ramage

    发明人： Alastair Hay ,  Graham Cotton ,  Robert Ramage

    IPC分类号： C07D401/00

    CPC分类号： C07K1/13 ,  C07D213/38

    摘要： Disclosed is a tag for purification of peptides. The tag structure facilitates the easy cleavage of a bond formed between the tag molecule and a peptide to which it is bound under conditions which minimize, indeed preferably prevent, damage to the peptide. The tag molecules of the invention may be used to separate and/or purify a peptide from a mixture of peptides and/or other components.

    摘要翻译： 公开了用于纯化肽的标签。 在最小化，实际上优选地防止对肽损伤的条件下，标签结构有助于容易地切割标签分子与其所结合的肽之间形成的键。 本发明的标签分子可用于从肽和/或其它组分的混合物分离和/或纯化肽。

    Protected compound comprising a protective group removably attached to a compound to be protected
    7.
    发明授权
    Protected compound comprising a protective group removably attached to a compound to be protected 失效
    保护性化合物，其包含可去除地连接到待保护化合物的保护基团

    公开(公告)号：US5869605A

    公开(公告)日：1999-02-09

    申请号：US288771

    申请日：1994-08-11

    申请人： Robert Ramage ,  Gilles Raphy

    发明人： Robert Ramage ,  Gilles Raphy

    IPC分类号： C07K1/06

    CPC分类号： C07K1/064 ,  C07K1/063 ,  Y02P20/55

    摘要： The protective group having the following formula (I):Ar--L-- (I)whereinAr represents a substantially planar, fused ring system containing at least 4 aromatic rings, andL represents a group containing at least one carbon atom which is capable of bonding to a group to be protected.

    摘要翻译： 具有下式（I）的保护基：Ar-L-（I）其中Ar表示包含至少4个芳环的基本上平面的稠环体系，L表示含有至少一个碳原子的基团，其能够 粘合到要保护的组。

    Process for the preparation of thiophenes
    9.
    发明授权
    Process for the preparation of thiophenes 失效
    制备噻吩的方法

    公开(公告)号：US4252976A

    公开(公告)日：1981-02-24

    申请号：US926727

    申请日：1978-07-21

    申请人： Angela W. Guest ,  Andrew W. Taylor ,  Robert Ramage

    发明人： Angela W. Guest ,  Andrew W. Taylor ,  Robert Ramage

    IPC分类号： C07C45/00 ,  C07C57/52 ,  C07C67/00 ,  C07C69/65 ,  C07C231/00 ,  C07C231/12 ,  C07C233/09 ,  C07C235/28 ,  C07C253/00 ,  C07C255/10 ,  C07D333/24

    CPC分类号： C07C255/00 ,  C07C45/00 ,  C07C57/52 ,  C07D333/24

    摘要： A process for the preparation of 3-substituted thiophenes which involves cyclization of a novel intermediate, avoids the use of previously employed expensive starting materials. The thiophenes are useful for the preparation of penicillins and cephalosporins.The process is for the preparation of a thiophene of formula (I): ##STR1## where R.sup.1 represents a carboxylic acid group, or an ester or amide thereof or a nitrile group; R.sup.2 represents a group suitable for use as an .alpha.-substituent in the side-chain of a penicillin or cephalosporin; which comprises treating a compound of formula (II): ##STR2## wherein X represents halogen or optionally functionalized hydroxyl, Y represents halogen, hydroxyl, or alkoxy; with a source of nucleophilic sulphur under basic conditions.

    摘要翻译： 制备3-取代噻吩的方法，其涉及新型中间体的环化，避免使用先前使用的昂贵起始原料。 噻吩可用于制备青霉素和头孢菌素。 该方法用于制备式（I）的噻吩：其中R 1表示羧酸基团，或其酯或酰胺或腈基; R2表示适合用作青霉素或头孢菌素的侧链中的α-取代基的基团; 其包括处理式（II）的化合物：其中X表示卤素或任选官能化的羟基，Y表示卤素，羟基或烷氧基; 在基本条件下具有亲核硫源。