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1. 发明授权

US11485744B2 High penetration prodrug compositions of antimicrobials and antimicrobial-related compounds 有权
公开(公告)号：US11485744B2
公开(公告)日：2022-11-01
申请号：US15947983
申请日：2018-04-09
申请人： Techfields Pharma Co., Ltd.
发明人： Chongxi Yu , Lina Xu , Yuhua Chen , Binbing Yan , Shiqian Tu
IPC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.

2. 发明申请

US20220096370A1 HIGH PENETRATION COMPOSITION AND USES THEREOF 有权
公开(公告)号：US20220096370A1
公开(公告)日：2022-03-31
申请号：US17493321
申请日：2021-10-04
申请人： TECHFIELDS PHARMA CO., LTD
发明人： Chongxi Yu , Lina Xu
IPC分类号： A61K9/00 , C07C233/25 , A61K31/22 , C07C231/12 , A61K47/54 , A61K9/70 , A61K31/167 , A61K31/612
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.

3. 发明授权

US09567329B2 High penetration prodrug compositions of 1H-imidazo[4,5-c]quinolin-4-amines and 1H-imidazo[4,5-c]quinolin-4-amine-related compounds and uses thereof 有权
标题翻译： 1H-咪唑并[4,5-c]喹啉-4-胺和1H-咪唑并[4,5-c]喹啉-4-胺相关化合物的高渗透前药组合物及其用途
公开(公告)号：US09567329B2
公开(公告)日：2017-02-14
申请号：US13732256
申请日：2012-12-31
申请人： Techfields Pharma Co., Ltd
发明人： Chongxi Yu
IPC分类号： C07D471/00 , A61K31/44 , A61K31/4745 , C07D471/04 , A61K9/00
CPC分类号： C07D471/04 , A61K9/0014 , A61K31/44 , A61K31/4745
摘要： The invention provides compositions of novel high penetration compositions (HPC) or high penetration prodrugs (HPP) of 1H-imidazo[4,5-c]quinolin-4-amines and 1H-imidazo[4,5-c]quinolin-4-amine-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.
摘要翻译：本发明提供了1H-咪唑并[4,5-c]喹啉-4-胺和1H-咪唑并[4,5-c]喹啉-4-胺的新型高渗透组合物（HPC）或高渗透前药（HPP）胺相关化合物，其能够穿过具有高穿透效率的生物屏障。 HPP在穿过生物屏障后能够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，HPP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。

4. 发明申请

US20230097823A1 HIGH PENETRATION PRODRUG COMPOSITIONS OF MUSTARDS AND MUSTARD-RELATED COMPOUNDS 有权
公开(公告)号：US20230097823A1
公开(公告)日：2023-03-30
申请号：US18049041
申请日：2022-10-24
申请人： TECHFIELDS PHARMA CO., LTD.
发明人： Chongxi Yu , Lina Xu
IPC分类号： 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.

5. 发明授权

US10233198B2 Pro-drugs of NSAIAs with very high skin and membranes penetration rates and their new medicinal uses 有权
公开(公告)号：US10233198B2
公开(公告)日：2019-03-19
申请号：US15165803
申请日：2016-05-26
申请人： Techfields Pharma Co., Ltd.
发明人： Chongxi Yu , Lina Xu
IPC分类号： C07D211/22 , C07D205/04 , C07D487/04 , C07D413/12 , C07D513/04 , C07D409/12 , C07D405/12 , C07D403/12 , C07D401/12 , C07D417/12 , C07D295/088 , 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.

6. 发明申请

US20170209585A1 HIGH PENETRATION COMPOSITIONS AND USES THEREOF 审中-公开
公开(公告)号：US20170209585A1
公开(公告)日：2017-07-27
申请号：US15402575
申请日：2017-01-10
申请人： Techfields Pharma Co., Ltd.
发明人： Chongxi Yu , Lina XU
IPC分类号： A61K49/00 , A61K31/24 , A61K9/00 , A61K9/70 , A61K47/48
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.

7. 发明申请

US20210353579A1 HIGH PENETRATION COMPOSITIONS AND USES THEREOF 有权
公开(公告)号：US20210353579A1
公开(公告)日：2021-11-18
申请号：US16421735
申请日：2019-05-24
申请人： Techfields Pharma Co., Ltd.
发明人： Chongxi Yu , Lina XU
IPC分类号： A61K31/216 , A61K9/00 , A61K9/70 , A61K31/24 , A61L15/44 , A61K47/54
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.

8. 发明申请

US20170334908A1 NOVEL HIGH PENETRATION DRUGS AND THEIR COMPOSITIONS THEREOF FOR TREATMENT OF PARKINSON DISEASES 审中-公开
公开(公告)号：US20170334908A1
公开(公告)日：2017-11-23
申请号：US15634272
申请日：2017-06-27
申请人： Techfields Pharma Co., Ltd.
发明人： Chongxi Yu , Lina XU
IPC分类号： C07D471/04 , C07D211/62 , C07D207/16 , C07C327/30 , C07C317/44 , C07C271/16 , C07C217/60 , C07C237/20 , C07C237/08 , C07C229/58 , C07C229/36 , C07C219/10 , C07D321/12 , C07C271/22
CPC分类号： C07D471/04 , A61K31/137 , A61K31/195 , A61K31/197 , A61K31/198 , A61K31/24 , A61K31/277 , A61K31/40 , C07C217/60 , C07C219/06 , C07C219/10 , C07C219/14 , C07C219/28 , C07C219/32 , C07C229/12 , C07C229/36 , C07C229/58 , C07C237/06 , C07C237/08 , C07C237/20 , C07C271/16 , C07C271/22 , C07C317/44 , C07C327/30 , C07C327/36 , C07C2602/08 , C07D207/16 , C07D211/62 , C07D321/12 , C07D455/02 , C07K5/0806 , C07K5/0823 , A61K2300/00
摘要： One aspect of the invention provides a composition of novel high penetration compositions (HPC) or a high penetration prodrug (HPP) for treatment of Parkinson's disease. 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.

9. 发明授权

US09718766B2 High penetration drugs and their compositions thereof for treatment of parkinson diseases 有权
公开(公告)号：US09718766B2
公开(公告)日：2017-08-01
申请号：US14854616
申请日：2015-09-15
申请人： Techfields Pharma Co., Ltd.
发明人： Chongxi Yu , Lina Xu
IPC分类号： A61K31/195 , C07C219/06 , C07C317/44 , A61K31/137 , C07C229/36 , A61K31/198 , A61K31/277 , C07C271/16 , C07C271/22 , C07D321/12 , C07C219/10 , C07C219/14 , C07C219/28 , C07C229/12 , C07C327/30 , C07C229/58 , C07D455/02 , C07D471/04 , C07C237/06 , C07C237/20 , C07D207/16 , C07K5/083 , C07D211/62 , C07K5/097 , A61K31/197 , A61K31/24 , A61K31/40 , C07C219/32 , C07C237/08 , C07C327/36
CPC分类号： C07D471/04 , A61K31/137 , A61K31/195 , A61K31/197 , A61K31/198 , A61K31/24 , A61K31/277 , A61K31/40 , C07C217/60 , C07C219/06 , C07C219/10 , C07C219/14 , C07C219/28 , C07C219/32 , C07C229/12 , C07C229/36 , C07C229/58 , C07C237/06 , C07C237/08 , C07C237/20 , C07C271/16 , C07C271/22 , C07C317/44 , C07C327/30 , C07C327/36 , C07C2602/08 , C07D207/16 , C07D211/62 , C07D321/12 , C07D455/02 , C07K5/0806 , C07K5/0823 , A61K2300/00
摘要： One aspect of the invention provides a composition of novel high penetration compositions (HPC) or a high penetration prodrug (HPP) for treatment of Parkinson's disease. 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.

10. 发明申请

US20230130980A1 HIGH PENETRATION PRODRUG COMPOSITIONS OF ANTIMICROBIALS AND ANTIMICROBIAL-RELATED COMPOUNDS 有权
公开(公告)号：US20230130980A1
公开(公告)日：2023-04-27
申请号：US18051060
申请日：2022-10-31
申请人： TECHFIELDS PHARMA CO., LTD.
发明人： Chongxi Yu , Lina Xu , Yuhua Chen , Binbing Yan , Shiqian Tu
IPC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.

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