公开(公告)号：US11351126B2

公开(公告)日：2022-06-07

申请号：US16633979

申请日：2018-07-26

申请人： BioMendics, LLC

发明人： Karen M. McGuire ,  Chun-che Tsai ,  Emily L. Plocinik ,  Aleesha M. McCormick

IPC分类号： A61K31/05 ,  A61P31/04 ,  A61K35/741

摘要： Described are methods for disinfecting a physical or biological surface by contact with an antimicrobial formulation comprising a substituted tolan compound, the substitutions being, for example, one or more alkoxy, (e.g., methoxy) and hydroxy substituents at one or both phenyl rings of the tolan. The compounds and methods are -static and/or -cidal, depending on dose and suspected microbe. Suspected pathogenic microbes include Gram negative bacteria, such as P. aeruginosa and E. coli, Gram positive bacteria, such as S. aureus, including MRSA, and fungal pathogens, such as Candida genus and C. albicans. Also described are methods for inhibiting or disrupting biofilm formation of a microbe or microbes.

公开(公告)号：US20200016096A1

公开(公告)日：2020-01-16

申请号：US16584195

申请日：2019-09-26

申请人： BioMendics, LLC

发明人： Chun-che Tsai ,  Karen M. McGuire ,  James M. Jamison ,  Jack L. Summers

IPC分类号： A61K31/05 ,  A61K31/655 ,  A61K31/375 ,  A61K31/167 ,  A61K31/03 ,  A61K8/73 ,  A61K8/70 ,  A61K9/19 ,  A61K9/08 ,  A61K9/00 ,  A61K8/67 ,  A61K8/60 ,  A61K8/33 ,  A61K8/34 ,  A61Q7/00 ,  A61Q19/08 ,  A61K47/40 ,  A61K47/36 ,  A61K9/06 ,  A61K45/06 ,  A61K31/7034 ,  A61K31/09 ,  A61K31/085

摘要： Methods and compounds are disclosed for wound healing by modulating autophagy. A formulation for modulating autophagy comprises a first modulating compound (FAM) selected from compounds having the general structure (I): wherein: L represents a linker selected from —C≡C—, (a tolan), —CH═CH— (a stilbene, preferably trans); or —CRa═CRb— a stilbene derivative; where Ra and Rb are independently H or phenyl optionally substituted with —(R3)p or —(R4)q; R1 to R4 are independent substituents at any available position of the phenyl rings, preferably at 3, 3′, 4, 4′, and/or 5, 5′; and m, n, p, and q are independently 0, 1, 2, or 3 representing the number of substituents of the rings, respectively, but at least one of m or n must be ≥1. Each R1 to R2 is independently selected from substituents described herein, including but not limited to hydroxyl, alkoxy, halo, halomethyl and glycosides. The formulation may also include an auxiliary autophagy modulating compound (AAM) as described herein. The formulation may include a hydrogel formed by the compounds themselves or otherwise and may include salts and/or complexes.

公开(公告)号：US20190022029A1

公开(公告)日：2019-01-24

申请号：US16058437

申请日：2018-08-08

申请人： BioMendics, LLC

发明人： Chun-che Tsai ,  Karen M. McGuire ,  James M. Jamison ,  Jack L. Summers

IPC分类号： A61K31/05 ,  A61K8/67 ,  A61K9/00 ,  A61K8/60 ,  A61K8/33 ,  A61K8/34 ,  A61Q7/00 ,  A61Q19/08 ,  A61K47/40 ,  A61K47/36 ,  A61K9/06 ,  A61K45/06 ,  A61K31/7034 ,  A61K31/09 ,  A61K31/085 ,  A61K8/73 ,  A61K9/08 ,  A61K9/19 ,  A61K8/70 ,  A61K31/03 ,  A61K31/167 ,  A61K31/375 ,  A61K31/655

CPC分类号： A61K31/05 ,  A61K8/33 ,  A61K8/347 ,  A61K8/602 ,  A61K8/676 ,  A61K8/70 ,  A61K8/733 ,  A61K8/738 ,  A61K9/0019 ,  A61K9/06 ,  A61K9/08 ,  A61K9/19 ,  A61K31/03 ,  A61K31/085 ,  A61K31/09 ,  A61K31/167 ,  A61K31/375 ,  A61K31/655 ,  A61K31/7034 ,  A61K45/06 ,  A61K47/36 ,  A61K47/40 ,  A61Q7/00 ,  A61Q19/08 ,  Y02A50/401 ,  A61K2300/00

摘要： Methods and compounds are disclosed for wound healing by modulating autophagy. A formulation for modulating autophagy comprises a first modulating compound (FAM) selected from compounds having the general structure (I): wherein: L represents a linker selected from —C≡C—, (a tolan), —CH═CH— (a stilbene, preferably trans); or —CRa═CRb— a stilbene derivative; where Ra and Rb are independently H or phenyl optionally substituted with —(R3)p or —(R4)q; R1 to R4 are independent substituents at any available position of the phenyl rings, preferably at 3, 3′, 4, 4′, and/or 5, 5′; and m, n, p, and q are independently 0, 1, 2, or 3 representing the number of substituents of the rings, respectively, but at least one of m or n must be ≥1. Each R1 to R2 is independently selected from substituents described herein, including but not limited to hydroxyl, alkoxy, halo, halomethyl and glycosides. The formulation may also include an auxiliary autophagy modulating compound (AAM) as described herein. The formulation may include a hydrogel formed by the compounds themselves or otherwise and may include salts and/or complexes.

公开(公告)号：US11786481B2

公开(公告)日：2023-10-17

申请号：US17221181

申请日：2021-04-02

申请人： BioMendics, LLC

发明人： Chun-che Tsai ,  Karen M. McGuire ,  James M. Jamison ,  Jack L. Summers

IPC分类号： A61K31/05 ,  A61K31/085 ,  A61K31/09 ,  A61K31/7034 ,  A61K45/06 ,  A61K9/06 ,  A61K47/36 ,  A61K47/40 ,  A61Q19/08 ,  A61Q7/00 ,  A61K8/34 ,  A61K8/33 ,  A61K8/60 ,  A61K8/73 ,  A61K8/67 ,  A61K9/00 ,  A61K9/08 ,  A61K9/19 ,  A61K8/70 ,  A61K31/03 ,  A61K31/167 ,  A61K31/375 ,  A61K31/655

CPC分类号： A61K31/05 ,  A61K8/33 ,  A61K8/347 ,  A61K8/602 ,  A61K8/676 ,  A61K8/70 ,  A61K8/733 ,  A61K8/738 ,  A61K9/0019 ,  A61K9/06 ,  A61K9/08 ,  A61K9/19 ,  A61K31/03 ,  A61K31/085 ,  A61K31/09 ,  A61K31/167 ,  A61K31/375 ,  A61K31/655 ,  A61K31/7034 ,  A61K45/06 ,  A61K47/36 ,  A61K47/40 ,  A61Q7/00 ,  A61Q19/08 ,  Y02A50/30 ,  A61K31/05 ,  A61K2300/00 ,  A61K31/03 ,  A61K2300/00 ,  A61K31/7034 ,  A61K2300/00 ,  A61K31/085 ,  A61K2300/00 ,  A61K31/09 ,  A61K2300/00 ,  A61K31/167 ,  A61K2300/00 ,  A61K31/655 ,  A61K2300/00

摘要： Methods and compounds are disclosed for wound healing by modulating autophagy. A formulation for modulating autophagy comprises a first modulating compound (FAM) selected from compounds having the general structure (I):






wherein: L represents a linker selected from —C≡C—, (a tolan), —CH═CH— (a stilbene, preferably trans); or —CRa═CRb— a stilbene derivative; where Ra and Rb are independently H or phenyl optionally substituted with —(R3)p or —(R4)q;
R1 to R4 are independent substituents at any available position of the phenyl rings, preferably at 3, 3′, 4, 4′, and/or 5, 5′; and m, n, p, and q are independently 0, 1, 2, or 3 representing the number of substituents of the rings, respectively, but at least one of m or n must be ≥1. Each R1 to R2 is independently selected from substituents described herein, including but not limited to hydroxyl, alkoxy, halo, halomethyl and glycosides. The formulation may also include an auxiliary autophagy modulating compound (AAM) as described herein. The formulation may include a hydrogel formed by the compounds themselves or otherwise and may include salts and/or complexes.

公开(公告)号：US20220296538A1

公开(公告)日：2022-09-22

申请号：US17833216

申请日：2022-06-06

申请人： BioMendics, LLC

发明人： Karen M. McGuire ,  Chun-che Tsai ,  Emily L. Plocinik ,  Aleesha M. McCormick

IPC分类号： A61K31/05 ,  A61P31/04 ,  A61K35/741

摘要： Described are methods for disinfecting a physical or biological surface by contact with an antimicrobial formulation comprising a substituted tolan compound, the substitutions being, for example, one or more alkoxy, (e.g., methoxy) and hydroxy substituents at one or both phenyl rings of the tolan. The compounds and methods are -static and/or -cidal, depending on dose and suspected microbe. Suspected pathogenic microbes include Gram negative bacteria, such as P. aeruginosa and E. coli, Gram positive bacteria, such as S. aureus, including MRSA, and fungal pathogens, such as Candida genus and C. albicans. Also described are methods for inhibiting or disrupting biofilm formation of a microbe or microbes.

公开(公告)号：US20210228501A1

公开(公告)日：2021-07-29

申请号：US17221181

申请日：2021-04-02

申请人： BioMendics, LLC

发明人： Chun-che Tsai ,  Karen M. McGuire ,  James M. Jamison ,  Jack L. Summers

IPC分类号： A61K31/05 ,  A61K31/085 ,  A61K31/09 ,  A61K31/7034 ,  A61K45/06 ,  A61K9/06 ,  A61K47/36 ,  A61K47/40 ,  A61Q19/08 ,  A61Q7/00 ,  A61K8/34 ,  A61K8/33 ,  A61K8/60 ,  A61K8/73 ,  A61K8/67 ,  A61K9/00 ,  A61K9/08 ,  A61K9/19 ,  A61K8/70 ,  A61K31/03 ,  A61K31/167 ,  A61K31/375 ,  A61K31/655

摘要： Methods and compounds are disclosed for wound healing by modulating autophagy. A formulation for modulating autophagy comprises a first modulating compound (FAM) selected from compounds having the general structure (I): wherein: L represents a linker selected from —C≡C—, (a tolan), —CH═CH— (a stilbene, preferably tram); or —CRa═CRb— a stilbene derivative; where Ra and Rb are independently H or phenyl optionally substituted with —(R3)p or —(R4)q; R1 to R4 are independent substituents at any available position of the phenyl rings, preferably at 3, 3′, 4, 4′, and/or 5, 5′; and m, n, p, and q are independently 0, 1, 2, or 3 representing the number of substituents of the rings, respectively, but at least one of m or n must be ≥1. Each R1 to R2 is independently selected from substituents described herein, including but not limited to hydroxyl, alkoxy, halo, halomethyl and glycosides. The formulation may also include an auxiliary autophagy modulating compound (AAM) as described herein. The formulation may include a hydrogel formed by the compounds themselves or otherwise and may include salts and/or complexes.

公开(公告)号：US20200206154A1

公开(公告)日：2020-07-02

申请号：US16633979

申请日：2018-07-26

申请人： BioMendics, LLC

发明人： Karen M. McGuire ,  Chun-che Tsai ,  Emily L. Plocinik ,  Aleesha M. McCormick

IPC分类号： A61K31/05 ,  A61K35/741 ,  A61P31/04

摘要： Described are methods for disinfecting a physical or biological surface by contact with an antimicrobial formulation comprising a substituted tolan compound, the substitutions being, for example, one or more alkoxy, (e.g., methoxy) and hydroxy substituents at one or both phenyl rings of the tolan. The compounds and methods are -static and/or -cidal, depending on dose and suspected microbe. Suspected pathogenic microbes include Gram negative bacteria, such as P. aeruginosa and E. coli, Gram positive bacteria, such as S. aureus, including MRSA, and fungal pathogens, such as Candida genus and C. albicans. Also described are methods for inhibiting or disrupting biofilm formation of a microbe or microbes.

公开(公告)号：US10426742B2

公开(公告)日：2019-10-01

申请号：US16058437

申请日：2018-08-08

申请人： BioMendics, LLC

发明人： Chun-che Tsai ,  Karen M. McGuire ,  James M. Jamison ,  Jack L. Summers

IPC分类号： A61K31/05 ,  A61K31/085 ,  A61K31/09 ,  A61K31/7034 ,  A61K45/06 ,  A61K9/06 ,  A61K47/36 ,  A61K47/40 ,  A61Q19/08 ,  A61Q7/00 ,  A61K8/34 ,  A61K8/33 ,  A61K8/60 ,  A61K8/73 ,  A61K8/67 ,  A61K9/00 ,  A61K9/08 ,  A61K9/19 ,  A61K8/70 ,  A61K31/03 ,  A61K31/167 ,  A61K31/375 ,  A61K31/655

摘要： Methods and compounds are disclosed for wound healing by modulating autophagy. A formulation for modulating autophagy comprises a first modulating compound (FAM) selected from compounds having the general structure (I): wherein: L represents a linker selected from —C≡C—, (a tolan), —CH═CH— (a stilbene, preferably trans); or —CRa═CRb— a stilbene derivative; where Ra and Rb are independently H or phenyl optionally substituted with —(R3)p or —(R4)q; R1 to R4 are independent substituents at any available position of the phenyl rings, preferably at 3, 3′, 4, 4′, and/or 5, 5′; and m, n, p, and q are independently 0, 1, 2, or 3 representing the number of substituents of the rings, respectively, but at least one of m or n must be ≥1. Each R1 to R2 is independently selected from substituents described herein, including but not limited to hydroxyl, alkoxy, halo, halomethyl and glycosides. The formulation may also include an auxiliary autophagy modulating compound (AAM) as described herein. The formulation may include a hydrogel formed by the compounds themselves or otherwise and may include salts and/or complexes.

公开(公告)号：US10045950B2

公开(公告)日：2018-08-14

申请号：US15093146

申请日：2016-04-07

申请人： BioMendics, LLC

发明人： Chun-che Tsai ,  Karen M. McGuire ,  James M. Jamison ,  Jack L. Summers

IPC分类号： A61K31/00 ,  A61K31/05 ,  A61K31/085 ,  A61K31/09 ,  A61K31/7034 ,  A61K45/06 ,  A61K9/06 ,  A61K47/36 ,  A61K47/40 ,  A61Q19/08 ,  A61Q7/00 ,  A61K8/34 ,  A61K8/33 ,  A61K8/60 ,  A61K8/73 ,  A61K8/67 ,  A61K9/00 ,  A61K9/08 ,  A61K9/19 ,  A61K8/70 ,  A61K31/03 ,  A61K31/167 ,  A61K31/375 ,  A61K31/655

摘要： Methods and compounds are disclosed for wound healing by modulating autophagy. A formulation for modulating autophagy comprises a first modulating compound (FAM) selected from compounds having the general structure (I): wherein: L represents a linker selected from —C≡C—, (a tolan), —CH═CH— (a stilbene, preferably trans); or —CRa═CRb— a stilbene derivative; where Ra and Rb are independently H or phenyl optionally substituted with —(R3)p or —(R4)q; R1 to R4 are independent substituents at any available position of the phenyl rings, preferably at 3, 3′, 4, 4′, and/or 5, 5′; and m, n, p, and q are independently 0, 1, 2, or 3 representing the number of substituents of the rings, respectively, but at least one of m or n must be ≥1. Each R1 to R2 is independently selected from substituents described herein, including but not limited to hydroxyl, alkoxy, halo, halomethyl and glycosides. The formulation may also include an auxiliary autophagy modulating compound (AAM) as described herein. The formulation may include a hydrogel formed by the compounds themselves or otherwise and may include salts and/or complexes.

公开(公告)号：US20160296477A1

公开(公告)日：2016-10-13

申请号：US15093146

申请日：2016-04-07

申请人： BioMendics, LLC

发明人： Chun-che Tsai ,  Karen M. McGuire ,  James M. Jamison ,  Jack L. Summers

IPC分类号： A61K31/05 ,  A61K31/085 ,  A61K31/09 ,  A61K31/7034 ,  A61K45/06 ,  A61K9/06 ,  A61K47/36 ,  A61K47/40 ,  A61K47/48 ,  A61Q19/08 ,  A61Q7/00 ,  A61Q11/00 ,  A61Q19/00 ,  A61Q17/04 ,  A61Q19/06 ,  A61K8/34 ,  A61K8/33 ,  A61K8/60 ,  A61K8/04 ,  A61K8/73 ,  A61K8/67 ,  A61K31/047

CPC分类号： A61K31/05 ,  A61K8/33 ,  A61K8/347 ,  A61K8/602 ,  A61K8/676 ,  A61K8/70 ,  A61K8/733 ,  A61K8/738 ,  A61K9/0019 ,  A61K9/06 ,  A61K9/08 ,  A61K9/19 ,  A61K31/03 ,  A61K31/085 ,  A61K31/09 ,  A61K31/167 ,  A61K31/375 ,  A61K31/655 ,  A61K31/7034 ,  A61K45/06 ,  A61K47/36 ,  A61K47/40 ,  A61Q7/00 ,  A61Q19/08 ,  Y02A50/401 ,  A61K2300/00

摘要： Methods and compounds are disclosed for wound healing by modulating autophagy. A formulation for modulating autophagy comprises a first modulating compound (FAM) selected from compounds having the general structure (I): wherein: L represents a linker selected from —C≡C—, (a tolan), —CH═CH— (a stilbene, preferably trans); or —CRa═CRb— a stilbene derivative; where Ra and Rb are independently H or phenyl optionally substituted with —(R3)p or —(R4)q; R1 to R4 are independent substituents at any available position of the phenyl rings, preferably at 3, 3′, 4, 4′, and/or 5, 5′; and m, n, p, and q are independently 0, 1, 2, or 3 representing the number of substituents of the rings, respectively, but at least one of m or n must be ≧1. Each R1 to R2 is independently selected from substituents described herein, including but not limited to hydroxyl, alkoxy, halo, halomethyl and glycosides. The formulation may also include an auxiliary autophagy modulating compound (AAM) as described herein. The formulation may include a hydrogel formed by the compounds themselves or otherwise and may include salts and/or complexes.

摘要翻译： 公开了通过调节自噬的伤口愈合的方法和化合物。 用于调节自噬的制剂包括选自具有一般结构（I）的化合物的第一调节化合物（FAM），其中：L表示选自-C≡C-，（甲氧基），-CH = CH-（二苯乙烯 ，优选反式）; 或-CRa = CRb-二苯乙烯衍生物; 其中R a和R b独立地为H或任选被 - （R 3）p或 - （R 4）q取代的苯基; R 1至R 4在苯环的任何可用位置是独立的取代基，优选3'，4'，4'和/或5'; m，n，p和q分别独立为0,1,2或3，表示环的取代基数，但m或n中的至少一个必须≥1。 每个R 1至R 2独立地选自本文所述的取代基，包括但不限于羟基，烷氧基，卤素，卤代甲基和糖苷。 制剂还可以包括如本文所述的辅助自噬调节化合物（AAM）。 制剂可以包括由化合物本身或其它物质形成的水凝胶，并且可以包括盐和/或配合物。