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    High penetration prodrug compositions of antimicrobials and antimicrobial-related compounds
    2.
    发明授权
    High penetration prodrug compositions of antimicrobials and antimicrobial-related compounds 有权

    公开(公告)号：US09969751B2

    公开(公告)日：2018-05-15

    申请号：US13323556

    申请日：2011-12-12

    申请人： Chongxi Yu ,  Lina Xu ,  Yuhua Chen ,  Binbing Yan ,  Shiqian Tu

    发明人： Chongxi Yu ,  Lina Xu ,  Yuhua Chen ,  Binbing Yan ,  Shiqian Tu

    IPC分类号： C07D499/21

    CPC分类号： C07D499/21

    摘要： The invention provides compositions of novel high penetration compositions (HPC) or high penetration prodrugs (HPP) of antimicrobials and antimicrobial-related compounds, which are capable of crossing biological barriers with high penetration efficiency. The HPCs/HPPs are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, the HPPs are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPCs/HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.

    HIGH PENETRATION PRODRUG COMPOSITIONS OF PEPTIDES AND PEPTIDE-RELATED COMPOUNDS
    4.
    发明申请
    HIGH PENETRATION PRODRUG COMPOSITIONS OF PEPTIDES AND PEPTIDE-RELATED COMPOUNDS 有权
    肽和肽相关化合物的高渗透性原料组合物

    公开(公告)号：US20120156279A1

    公开(公告)日：2012-06-21

    申请号：US13291904

    申请日：2011-11-08

    申请人： Chongxi Yu ,  Lina Xu ,  Yuhua Chen ,  Binbing Yan ,  Shiqian Tu

    发明人： Chongxi Yu ,  Lina Xu ,  Yuhua Chen ,  Binbing Yan ,  Shiqian Tu

    IPC分类号： A61K9/70

    CPC分类号： A61K31/145 ,  A61K9/0014 ,  A61K31/222 ,  A61K31/40 ,  A61K31/4184 ,  A61K38/00 ,  A61K47/42 ,  A61K47/54 ,  A61K47/64 ,  A61K47/645 ,  C07D403/12 ,  C07D403/14 ,  C07K1/04 ,  C07K5/06026 ,  C07K5/06078 ,  C07K5/1013 ,  C07K5/1016 ,  C07K5/1019 ,  C07K7/06 ,  C07K7/56

    摘要： The invention provides compositions of novel high penetration compositions (HPC) or high penetration prodrugs (HPP) of peptides and peptide-related compounds, which are capable of crossing biological barriers with higher penetration efficiency comparing to their parent drugs. The HPPs are capable of being converted to parent drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, the HPPs/HPCs are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPPs/HPCs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.

    摘要翻译： 本发明提供了肽和肽相关化合物的新型高渗透组合物（HPC）或高渗透前药（HPP）的组合物，其能够与其母体药物相比具有更高穿透效率的生物屏障。 HPP在穿过生物屏障后能够转化为母体药物或药物代谢物，因此可以对母体药物或代谢物可以进行的处理。 此外，HPP / HPC能够达到母体药物可能无法进入或在目标区域提供足够浓度的区域，从而进行新的治疗。 HPP / HPC可以通过各种施用途径施用于受试者，例如局部递送至具有高浓度或系统地施用于生物学受试者的病症的作用部位并以更快的速率进入总体循环。

    HIGH PENETRATION COMPOSITIONS AND USES THEREOF
    5.
    发明申请
    HIGH PENETRATION COMPOSITIONS AND USES THEREOF 审中-公开
    高渗透组合物及其用途

    公开(公告)号：US20090238763A1

    公开(公告)日：2009-09-24

    申请号：US12351804

    申请日：2009-01-09

    申请人： Chongxi Yu ,  Lina Xu

    发明人： Chongxi Yu ,  Lina Xu

    IPC分类号： A61K31/625 ,  A61K31/60 ,  A61B10/00 ,  A61P9/10 ,  A61P9/04 ,  A61P9/12 ,  A61P25/28 ,  A61P25/16 ,  A61P37/02 ,  A61P19/02 ,  A61P29/00 ,  A61P17/06 ,  A61P17/10 ,  A61P17/00 ,  A61P35/00 ,  A61P35/02 ,  A61P19/10 ,  A61P19/08

    CPC分类号： A61K31/216 ,  A61K9/0014 ,  A61K9/0043 ,  A61K9/0073 ,  A61K9/703 ,  A61K31/24 ,  A61K47/54 ,  A61L15/44 ,  A61L2300/21

    摘要： The present invention relates to compositions and uses of novel high penetration compositions or high penetration prodrugs (HPP), in particular HPPs for non-steroidal anti-inflammatory agents (NSAIAs), which are capable of crossing biological barriers with high penetration efficiency. The HPPs herein are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, due to the ability of penetrating biological barriers, the HPPs herein are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPPs herein can be administered to a subject through various administration routes. For example, the HPPs can be locally delivered to an action site of a condition with a high concentration due to their ability of penetrating biological barriers and thus obviate the need for a systematic administration. For another example, the HPPs herein can be systematically administer to a biological subject and enter the general circulation with a faster rate.

    摘要翻译： 本发明涉及新型高渗透组合物或高渗透性前药（HPP），特别是用于非甾体抗炎剂（NSAIA）的HPP的组合物和用途，其能够以高渗透效率穿过生物屏障。 本文中的HPP能够在穿过生物屏障之后转化为亲本活性药物或药物代谢物，因此可以对母体药物或代谢物可以进行的处理。 此外，由于穿透生物屏障的能力，本文的HPP能够达到母体药物可能无法进入或在目标区域呈现足够浓度的区域，因此进行新的治疗。 这里的HPP可以通过各种管理途径施用于受试者。 例如，HPP可以由于其穿透生物屏障的能力而被局部递送到具有高浓度的病症的动作部位，从而避免了对系统性给药的需要。 另一个例子，这里的HPP可以系统地施用于生物受试者并以更快的速率进入总体循环。

    High penetration prodrug compositions of mustards and mustard-related compounds
    6.
    发明授权
    High penetration prodrug compositions of mustards and mustard-related compounds 有权

    公开(公告)号：US10189774B2

    公开(公告)日：2019-01-29

    申请号：US12418564

    申请日：2009-04-03

    申请人： Chongxi Yu ,  Lina Xu

    发明人： Chongxi Yu ,  Lina Xu

    IPC分类号： A61K31/661 ,  A61P35/00 ,  C07C233/47 ,  C07C229/42 ,  C07F9/24

    摘要： The invention provides compositions of novel high penetration compositions (HPC) or high penetration prodrugs (HPP) of mustards and mustard-related compounds, which are capable of crossing biological barriers with high penetration efficiency. The HPPs are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, the HPPs are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.

    HIGH PENETRATION COMPOSITION AND USES THEREOF
    7.
    发明申请
    HIGH PENETRATION COMPOSITION AND USES THEREOF 审中-公开
    高渗透组合物及其用途

    公开(公告)号：US20090221703A1

    公开(公告)日：2009-09-03

    申请号：US12397308

    申请日：2009-03-03

    申请人： Chongxi Yu ,  Lina Xu

    发明人： Chongxi Yu ,  Lina Xu

    IPC分类号： A61K31/22 ,  C07C229/02 ,  A61P37/06 ,  A61P29/00 ,  A61P25/00

    CPC分类号： A61K9/0014 ,  A61K9/7023 ,  A61K31/167 ,  A61K31/22 ,  A61K31/612 ,  A61K47/54 ,  A61K47/542 ,  C07C231/12 ,  C07C233/25

    摘要： The present invention relates to compositions and uses of novel high penetration compositions or high penetration prodrugs (HPP), in particular HPPs for 4-aminophenol derivatives, which are capable of crossing biological barriers with high penetration efficiency. The HPPs herein are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, due to the ability of penetrating biological barriers, the HPPs herein are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPPs herein can be administered to a subject through various administration routes. For example, the HPPs can be locally delivered to an action site of a condition with a high concentration due to their ability of penetrating biological barriers and thus obviate the need for a systematic administration. For another example, the HPPs herein can be systematically administer to a biological subject and enter the general circulation with a faster rate.

    摘要翻译： 本发明涉及新型高渗透组合物或高渗透性前药（HPP），特别是4-氨基苯酚衍生物的HPP的组合物和用途，其能够穿透具有高穿透效率的生物屏障。 本文中的HPP能够在穿过生物屏障之后转化为亲本活性药物或药物代谢物，因此可以对母体药物或代谢物可以进行的处理。 此外，由于穿透生物屏障的能力，本文的HPP能够达到母体药物可能无法进入或在目标区域呈现足够浓度的区域，因此进行新的治疗。 这里的HPP可以通过各种管理途径施用于受试者。 例如，HPP可以由于其穿透生物屏障的能力而被局部递送到具有高浓度的病症的动作部位，从而避免了对系统性给药的需要。 另一个例子，这里的HPP可以系统地施用于生物受试者并以更快的速率进入总体循环。

    High penetration prodrug compositions of prostaglandins and related compounds
    8.
    发明授权
    High penetration prodrug compositions of prostaglandins and related compounds 有权

    公开(公告)号：US11555014B2

    公开(公告)日：2023-01-17

    申请号：US12417621

    申请日：2009-04-02

    申请人： Chongxi Yu ,  Lina Xu

    发明人： Chongxi Yu ,  Lina Xu

    IPC分类号： C07C405/00

    摘要： The invention provides compositions of novel high penetration compositions (HPC) or high penetration prodrugs (HPP) of prostaglandins or prostaglandin analogs which are capable of crossing biological barriers with high penetration efficiency. The HPPs are capable of being converted to parent prostaglandins or prostaglandin analogs after crossing the biological barrier and thus can render treatments for the conditions that the parent prostaglandins or prostaglandin analogs can. Additionally, the HPPs are capable of reaching areas that parent prostaglandins or prostaglandin analogs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.

    Pro-drugs of NSAIAS with very high skin and membranes penetration rates and their new medicinal uses
    9.
    发明授权
    Pro-drugs of NSAIAS with very high skin and membranes penetration rates and their new medicinal uses 有权

    公开(公告)号：US09371284B2

    公开(公告)日：2016-06-21

    申请号：US12663262

    申请日：2007-06-04

    申请人： Chongxi Yu ,  Lina Xu

    发明人： Chongxi Yu ,  Lina Xu

    IPC分类号： A61K31/397 ,  A61K9/70 ,  C07D229/00 ,  C07D405/02 ,  C07D513/04 ,  A61P17/00 ,  C07D211/22 ,  C07D295/088

    CPC分类号： C07D513/04 ,  C07D205/04 ,  C07D211/22 ,  C07D295/088 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D487/04 ,  C07D491/052

    摘要： The novel positively charged pro-drugs of NSAIAs in the general formulas (1, 2a, 2b, 2c, or 2d) “Structure 1, 2a, 2b, 2c, or 2d” were designed and synthesized. The compounds of the general formulas (1, 2a, 2b, 2c, or 2d) “Structure 1, 2a, 2b, 2c, or 2d” indicated above can be prepared from metal salts, organic base salts, or immobilized base salts of NSAIAs with suitable halide compounds. The positively charged amino groups in the pro-drugs in this invention largely increase the solubility of the drugs in water and will bond to the negative charge on the phosphate head group of membrane. Thus, the local concentration of the outside of the membrane or skin will be very high and will facilitate the passage of these pro-drugs from a region of high concentration to a region of low concentration. This bonding will disturb the membrane a little bit and may make some room for the lipophilic portion of the pro-drug. When the molecules of membrane move, the membrane may “crack” a little bit due to the bonding of the pro-drug. This will let the pro-drug insert into the membrane. At pH 7.4, only about 99% of the amino group is protonated. When the amino group is not protonated, the bonding between the amino group of the pro-drug and the phosphate head group of the membrane will disassociate, and the pro-drug will enter the membrane completely. When the amino group of the pro-drug flips to the other side of the membrane and thus becomes protonated, then the pro-drug is pulled into the cytosol, a semi-liquid concentrated aqueous solution or suspension. These pro-drugs can be used for treating and preventing diabetes (type I or/and type II), abnormal blood glucose and lipid levels, stroke, heart attack, and other heart and vascular diseases Alzheimer's diseases, Parkinson's diseases and other neurodegenerative diseases, psoriasis, discoid lupus erythematosus, systemic lupus erythematosus (SLE), autoimmune hepatitis, multiple sclerosis (MS), and other autoimmune diseases, amyotrophic lateral sclerosis (ALS), oculopharyngeal muscular dystrophy (OPMD), and other muscle disorders, inflamed hemorrhoids, cryptitis, other inflammatory conditions of the anorectum, and pruritus ani, prostatitis, prostatocystitis, varicose veins, autoimmune liver inflammation, autoimmune kidney inflammation, vein inflammation and other inflammations, skin cancers, breast cancer, colon-rectum cancer, oral cancer, and other cancers, scars, abnormal vascular skin lesions, birthmarks, moles (nevi), skin tags, aging spots (liver spots), and other skin disorders. These pro-drugs can be administered transdermally without the help of skin penetration enhancers.

    HIGH PENETRATION PRODRUG COMPOSITIONS OF PROSTAGLANDINS AND RELATED COMPOUNDS
    10.
    发明申请
    HIGH PENETRATION PRODRUG COMPOSITIONS OF PROSTAGLANDINS AND RELATED COMPOUNDS 审中-公开
    前列腺素和相关化合物的高渗透制剂组合物

    公开(公告)号：US20090252685A1

    公开(公告)日：2009-10-08

    申请号：US12417621

    申请日：2009-04-02

    申请人： Chongxi Yu ,  Lina Xu

    发明人： Chongxi Yu ,  Lina Xu

    IPC分类号： A61K49/00 ,  C07C405/00 ,  A61K31/19 ,  C07D317/44 ,  A61K31/335 ,  C07D307/77 ,  A61K31/343 ,  A61P15/00 ,  A61P9/12

    CPC分类号： C07C405/0041

    摘要： The invention provides compositions of novel high penetration compositions (HPC) or high penetration prodrugs (HPP) of prostaglandins or prostaglandin analogs which are capable of crossing biological barriers with high penetration efficiency. The HPPs are capable of being converted to parent prostaglandins or prostaglandin analogs after crossing the biological barrier and thus can render treatments for the conditions that the parent prostaglandins or prostaglandin analogs can. Additionally, the HPPs are capable of reaching areas that parent prostaglandins or prostaglandin analogs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.

    摘要翻译： 本发明提供能够跨越高渗透效率的生物屏障的前列腺素或前列腺素类似物的新型高渗透组合物（HPC）或高渗透前药（HPP）的组合物。 HPP在穿过生物屏障之后能够转化为母体前列腺素或前列腺素类似物，因此可以对母体前列腺素或前列腺素类似物的条件进行治疗。 此外，HPP能够达到母体前列腺素或前列腺素类似物可能无法进入或在目标区域产生足够浓度并因此进行新的治疗的区域。 HPP可以通过各种施用途径施用于受试者，例如局部递送至具有高浓度或系统地施用于生物受试者的病症的作用部位并以更快的速率进入总体循环。