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    AZABENZIMIDAZOLONES
    46.
    发明申请
    AZABENZIMIDAZOLONES 审中-公开

    公开(公告)号：US20110190336A1

    公开(公告)日：2011-08-04

    申请号：US13062794

    申请日：2009-10-14

    Applicant: Robert Zhiyong Luo ,  Mary-Margaret Zablocki

    Inventor： Robert Zhiyong Luo ,  Mary-Margaret Zablocki

    IPC: A61K31/437 ,  C07D471/04 ,  A61P25/00 ,  A61P29/00 ,  A61P37/08

    CPC classification number: C07D487/04 ,  C07D471/04

    Abstract: Compounds are provided having the general structure of formula I: In formula I, one member of the group (W, X, Y and Z) is a nitrogen atom and the remaining three members of the group are each independently a carbon atom covalently bonded to a radical, R4. The radicals, R1, R2, R3 and R4 are each defined herein, and n is an integer from 1 to 4. Also provided are stereoisomers, prodrugs, pharmaceutically acceptable salts, hydrates, salt hydrates, acid salt hydrates, and polymorphs of the compounds having the structure of formula I. The compounds bind the prostaglandin D2 receptor and are useful in the prophylaxis and treatment of prostaglandin D2-mediated diseases and conditions, including pain and inflammation, as well as asthma and allergic diseases and conditions.

    Abstract translation: 提供具有通式I的通式的化合物：在式I中，基团（W，X，Y和Z）中的一个成员为氮原子，其余三个基团各自独立地为与 一个激进的，R4。 基团，R 1，R 2，R 3和R 4各自如本文所定义，n是1至4的整数。还提供了化合物的立体异构体，前药，药学上可接受的盐，水合物，盐水合物，酸盐水合物和多晶型物 具有式I的结构。该化合物结合前列腺素D2受体并且可用于预防和治疗前列腺素D2介导的疾病和病症，包括疼痛和炎症，以及哮喘和过敏性疾病和病症。

    Synthetic peptide amides
    48.
    发明授权
    Synthetic peptide amides 有权
    合成肽酰胺

    公开(公告)号：US07402564B1

    公开(公告)日：2008-07-22

    申请号：US11938771

    申请日：2007-11-12

    Applicant: Claudio D. Schteingart ,  Frédérique Menzaghi ,  Guangcheng Jiang ,  Roberta Vezza Alexander ,  Javier Sueiras-Diaz ,  Robert H. Spencer ,  Derek T. Chalmers ,  Zhiyong Luo

    Inventor： Claudio D. Schteingart ,  Frédérique Menzaghi ,  Guangcheng Jiang ,  Roberta Vezza Alexander ,  Javier Sueiras-Diaz ,  Robert H. Spencer ,  Derek T. Chalmers ,  Zhiyong Luo

    IPC: A61K38/07

    CPC classification number: C07K5/1016 ,  A61K38/00 ,  A61K38/07 ,  C07K5/10 ,  C07K5/1008 ,  C07K5/101 ,  C07K7/02

    Abstract: The invention relates to synthetic peptide amide ligands of the kappa opioid receptor and particularly to agonists of the kappa opioid receptor that exhibit low P450 CYP inhibition and low penetration into the brain. The synthetic peptide amides of the invention conform to the structure of formula I: Pharmaceutical compositions containing these compounds are useful in the prophylaxis and treatment of pain and inflammation associated with a variety of diseases and conditions. Such treatable pain includes visceral pain, neuropathic pain and hyperalgesia. Inflammation associated with conditions such as IBD and IBS, ocular and otic inflammation, other disorders and conditions such as pruritis, edema, hyponatremia, hypokalemia, ileus, tussis and glaucoma are treatable or preventable with the pharmaceutical compositions of the invention.

    Abstract translation: 本发明涉及κ阿片样物质受体的合成肽酰胺配体，特别涉及表现出低P CYP抑制和低渗透入脑的κ阿片受体的激动剂。 本发明的合成肽酰胺符合式I的结构：含有这些化合物的药物组合物可用于预防和治疗与各种疾病和病症相关的疼痛和炎症。 这种可治疗的疼痛包括内脏痛，神经性疼痛和痛觉过敏。 与IBD和IBS等条件相关的炎症，眼部和耳部炎症，其他疾病和病症如瘙痒症，水肿，低钠血症，低钾血症，肠梗阻，肠炎和青光眼均可用本发明的药物组合物治疗或预防。

    Fluorous tin compounds an methods of using fluorous tin compounds
    49.
    发明授权
    Fluorous tin compounds an methods of using fluorous tin compounds 失效
    氟锡化合物是使用氟锡化合物的方法

    公开(公告)号：US06861544B1

    公开(公告)日：2005-03-01

    申请号：US09602105

    申请日：2000-06-22

    Applicant: Dennis P. Curran ,  Zhiyong Luo

    Inventor： Dennis P. Curran ,  Zhiyong Luo

    IPC: C07F7/22

    CPC classification number: C07F7/2224 ,  C07F7/2208

    Abstract: A method of carrying out a reaction comprising the steps of: mixing at least one organic reaction component with at least one fluorous reaction component having the formula: X1Sn(R)n[Rs(Rf)]3-n, X1X2Sn[Rs(Rf)]2 or O═Sn[Rs(Rf)]2 wherein n is 1 or 2, R is a C1-C6 alkyl group, X1 and X2 are independently, the same or different, H, F, Cl, Br, I, N3, OR1, OOR1 SR1, SeR1, CN, NC, NR1R2, an aryl group, a heteroaryl group, an alkyl group of 1 to 20 carbons, an alkenyl group, an alkynyl group, —C(O)R3, M((Rs′)(Rf′))3, OM((Rs′)(Rf′))3 or OOM((Rs′)Rf′))3, wherein M is Si, Ge, or Sn, and wherein R1 and R2 are each independently the same or different H, an alkyl group, —SO2R3 or —C(O)R3, wherein R3 is an alkyl group or an aryl group, and wherein Rs and Rs′ are each independently the same or different a spacer group, and wherein Rf and Rf′ are each independently the same or different a fluorous group; carrying out a reaction to produce an organic product; and after producing the organic product, separating any excess of the fluorous reaction component and any fluorous byproduct of the fluorous reaction component using a fluorous separation technique. Several compounds have the formula: X1Sn(R)n[Rs(Rf)3-n, X1X2Sn[Rs(Rf)]2 or O═Sn[Rs(Rf)]2.

    Abstract translation: 一种进行反应的方法，包括以下步骤：将至少一种有机反应组分与至少一种具有下式的氟反应组分混合：其中n是1或2，R是C 1 -C 6烷基，X 1， 和X 2独立地相同或不同，H，F，Cl，Br，I，N 3，OR 1，OOR 1 SR 1，SeR 1，CN，NC， R 2，芳基，杂芳基，碳原子数1〜20的烷基，烯基，炔基，-C（O）R 3，M（（R''）（Rf '））3，OM（（Rs'）（Rf'））3或OOM（（Rs'）Rf'））3，其中M是Si，Ge或Sn，其中R 1和R 2 各自独立地相同或不同，H，烷基，-SO 2 R 3或-C（O）R 3，其中R 3是烷基或芳基，并且其中R 5和R' 各自独立地相同或不同的间隔基，并且其中Rf和Rf'各自独立地相同或不同，含氟基团; 进行产生有机产物的反应; 在生产有机产物之后，使用氟分离技术分离氟反应组分和氟反应组分的任何氟副产物的任何过量。 几种化合物具有下式：

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