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1. 发明授权

US11286276B2 Cationic steroidal antimicrobials 有权
公开(公告)号：US11286276B2
公开(公告)日：2022-03-29
申请号：US15481884
申请日：2017-04-07
申请人： Paul B. Savage
发明人： Paul B. Savage
IPC分类号： C07J41/00
摘要： Disclosed herein are cationic steroidal antimicrobials (“CSA compounds” or “ceragenins”) and methods of making the same. Particularly advantageous methods are identified for the synthesis of CSA compounds. CSA compounds may be formulated for treating subjects with ailments responsive to CSA compounds, including but not limited to treating bacterial infections. Accordingly, some embodiments include formulations and methods of administering CSA compounds.

2. 发明申请

US20210363174A1 CATIONIC STEROIDAL ANTIMICROBIAL COMPOUNDS WITH ENDOGENOUS GROUPS 有权
公开(公告)号：US20210363174A1
公开(公告)日：2021-11-25
申请号：US17324329
申请日：2021-05-19
申请人： Paul B. Savage
发明人： Paul B. Savage
IPC分类号： C07J41/00
摘要： Cationic steroidal antimicrobial (CSA) compounds having a structure of Formula I, II or III, or salt thereof, wherein at least one of R1-R18, (e.g., R18) includes a terpenyl group attached via an ester or amide linkage and at least one R1-R18, (e.g., R3, R7 and R12) is an amino acid linked to the steroidal backbone by an ester or amide linkage: R18 has the following structure: —R19—(C═O)—X—R20 where R19 is omitted or alkyl, alkenyl, alkynyl, or aryl, X is oxygen or nitrogen, and R20 is a terpenyl group. R3, R7 and R12 have the following structure: R22R23N—R21—(C═O)—X— where R21 is substituted or unsubstituted alkyl, X is oxygen or nitrogen, and R22 and R23 are independently hydrogen, alkyl, alkenyl, alkynyl, or aryl.

3. 发明申请

US20210355155A1 CATIONIC STEROIDAL ANTIMICROBIAL COMPOUNDS WITH URETHANE LINKAGES 有权
公开(公告)号：US20210355155A1
公开(公告)日：2021-11-18
申请号：US17318206
申请日：2021-05-12
申请人： Paul B. Savage
发明人： Paul B. Savage
IPC分类号： C07J9/00
摘要： Cationic steroidal antimicrobial (CSA) compounds having a structure of Formula I, II or III, or salt thereof, wherein at least one of at least one of R1-R18, (e.g., R3, R7 and R12) is linked to the steroidal backbone by a urethane group: At least one of R1-R18, (e.g., R3, R7 and R12) has the following urethanyl structure: —O—(C═O)—NR19R20 where R19 and R20 are independently hydrogen, alkyl, alkenyl, alkynyl, aryl, aminoalkyl, aminoalkenyl, aminoalkynyl, or aminoaryl, provided that at least one of R19 or R20 includes an amino group (e.g., R19 is hydrogen and R20 is (C2-C6)aminoalkyl).
R18 can have the following structure: —R21—(C═O)—NR22R23 where R21 is omitted or alkyl, alkenyl, alkynyl, or aryl, and R22 and R23 are hydrogen, alkyl, alkenyl, alkynyl, or aryl, provided that at least one of R22 or R23 is not hydrogen.

4. 发明授权

US10959433B2 Use of cationic steroidal antimicrobials for sporicidal activity 有权
公开(公告)号：US10959433B2
公开(公告)日：2021-03-30
申请号：US15926534
申请日：2018-03-20
申请人： Paul B. Savage
发明人： Paul B. Savage
IPC分类号： A01N45/00 , A61L2/18 , A61P31/04 , A01N55/00 , A01N55/08 , A01N47/44 , A01N47/28
摘要： This disclosure relates to sporicidal compositions and uses thereof. The sporicidal compositions include one or more cationic steroidal antimicrobials (CSAs). The sporicidal compositions may be applied to an object to kill or deactivate bacterial spores contacting the sporicidal composition. The object may be a food product, food processing equipment, industrial equipment, or healthcare facility objects. The sporicidal composition may be administered to a subject that has, is suspected to have, or is at risk for an infection associated with spore-forming bacteria.

5. 发明授权

US10227376B2 Radiolabeled cationic steroid antimicrobials and diagnostic methods 有权
公开(公告)号：US10227376B2
公开(公告)日：2019-03-12
申请号：US14830356
申请日：2015-08-19
申请人： Paul B. Savage
发明人： Paul B. Savage
IPC分类号： G01N33/534 , C07J43/00 , A61K51/04 , C07J41/00 , G01N33/569
摘要： The disclosure provides compounds, methods, and kits for diagnosis, detection, screening, and imaging of a disease condition (e.g., infection, cancer, tumor, neoplasia), in vitro, ex vivo, and/or in vivo. Certain embodiments include administering a cationic steroid antimicrobial (a “CSA” or “ceragenin”), the CSA including a steroidal backbone and a heterocyclic ring separated from the steroidal backbone by at least 4 atoms (and up to 24 atoms or more), to a subject having or at risk of having a disease condition in an amount effective to diagnose, detect, screen for or image the disease condition in the subject.

6. 发明授权

US10195215B2 Methods for reducing cellular proliferation and treating certain diseases 有权
公开(公告)号：US10195215B2
公开(公告)日：2019-02-05
申请号：US15895848
申请日：2018-02-13
申请人： Carl Genberg , Paul B. Savage
发明人： Carl Genberg , Paul B. Savage
IPC分类号： A61K31/575 , A61K31/56
摘要： Disclosed herein are methods of treating cancer and/or reducing cellular proliferation in a patient, comprising identifying a patient in need of treatment and administering a therapeutically effective amount of at least one cationic steroid antimicrobial (CSA), or a pharmaceutically acceptable salt thereof. Kits comprising such compositions and instructions on such methods are also contemplated herein.

7. 发明申请

US20170174720A9 CATIONIC STEROIDAL ANTIMICROBIAL SALTS 审中-公开
公开(公告)号：US20170174720A9
公开(公告)日：2017-06-22
申请号：US15135928
申请日：2016-04-22
申请人： Paul B. Savage , Saurabh Shashikant Chitre , Kunal Arvind Varia , Hayley Ann Reece , Thomas E. Jacks , Ross A. Miller , Jared Lynn Randall
发明人： Paul B. Savage , Saurabh Shashikant Chitre , Kunal Arvind Varia , Hayley Ann Reece , Thomas E. Jacks , Ross A. Miller , Jared Lynn Randall
IPC分类号： C07J41/00 , C07C309/29 , C07C309/35
CPC分类号： C07J41/0088 , C07B2200/13 , C07C309/29 , C07C309/35 , C07J41/0061
摘要： Disclosed herein are acid addition salts of cationic steroidal antimicrobials (“CSAs” or “ceragenins”) and methods of making the same. Particularly advantageous salt forms are identified, such as 1,5-naphthalenedisulfonic acid addition salts and sulfate addition salts. The acid addition salts may be formulated for treating subjects with ailments responsive to CSAs, including but not limited to treating bacterial infections. Accordingly, some embodiments include formulations and methods of administering acid addition salts of CSAs.

8. 发明授权

US09603859B2 Methods and products for increasing the rate of healing of tissue wounds 有权
公开(公告)号：US09603859B2
公开(公告)日：2017-03-28
申请号：US14848819
申请日：2015-09-09
申请人： Carl Genberg , Paul B. Savage
发明人： Carl Genberg , Paul B. Savage
IPC分类号： A61K31/575
CPC分类号： A61K31/575
摘要： Disclosed are methods for increasing the rate of healing of a tissue wound by administering a composition including a therapeutically effective amount of at least one cationic steroid antimicrobial (CSA). Also disclosed herein are methods of promoting wound healing in a subject in need of such promotion, comprising administering a composition comprising a therapeutically effective amount of at least one CSA. Additionally, disclosed herein are compounds and compositions comprising at least one CSA, or a pharmaceutically acceptable salt thereof, for use in the treatment of a tissue wound. Kits comprising such compositions and instructions on such methods are also contemplated herein.

9. 发明申请

US20160311851A1 METHODS FOR THE SYNTHESIS OF CERAGENINS 审中-公开
公开(公告)号：US20160311851A1
公开(公告)日：2016-10-27
申请号：US15135969
申请日：2016-04-22
申请人： Paul B. Savage , Thomas E. Jacks , Ross A. Miller , Andrew S. Thompson , Jared Lynn Randall
发明人： Paul B. Savage , Thomas E. Jacks , Ross A. Miller , Andrew S. Thompson , Jared Lynn Randall
IPC分类号： C07J41/00
CPC分类号： C07J41/0088 , C07J9/005 , C07J41/0055 , C07J41/0061
摘要： Disclosed herein are methods of making ceragnenin compounds for treating, preventing, or diagnosing diseases, disorders, or conditions associated with bacterial or viral infections, cancer, inflammation, and osteogenesis. Ceragenin compounds display broad-spectrum antibacterial activity utilizing a mode of action similar to antimicrobial peptides, but without the high synthesis costs and susceptibility to proteolytic degradation. Ceragenin compounds reproduce the amphiphilic morphology found in many antimicrobial peptides and display potent and diverse biological activities, including anti-bacterial, anti-cancer, anti-inflammatory, bone growth promotion, and wound healing promotion.

10. 发明申请

US20160199390A1 ANIMAL FEED INCLUDING CATIONIC CHOLESTEROL ADDITIVE AND RELATED METHODS 审中-公开
标题翻译：动物饲料包括阳离子胆固醇添加剂和相关方法
公开(公告)号：US20160199390A1
公开(公告)日：2016-07-14
申请号：US15076313
申请日：2016-03-21
申请人： Chad S. Beus , Paul B. Savage
发明人： Chad S. Beus , Paul B. Savage
IPC分类号： A61K31/575 , A23K20/168
CPC分类号： A61K31/575 , A23K20/10 , A23K20/168 , A23K50/10 , A23K50/20 , A23K50/30 , A23K50/45 , A23K50/75 , A23V2002/00 , A23V2200/32
摘要： Methods and feed compositions for increasing health of agricultural animals incude administering a cationic cholesterol additive through the diet of the animal, such as through solid feed or drinking water of the animals. The method includes feeding an animal a diet comprised of a cationic cholesterol additive, such as a compound with a sterol backbone and a plurality of cationic groups attached thereto. The feed composition may include a solid or liquid feed component and a cationic cholesterol additive. The methods and compositions are useful for animals raised in confined feed operations, such as cattle, swine, horses, sheep, or poultry, and can reduce harmful bacteria in the digestive tract, increase beneficial bacteria flora, improve feed conversion efficiency, reduce morbity and/or mortality, and/or yield harvested meat having reduced content of harmful bacteria.
摘要翻译：用于增加农业动物健康的方法和饲料组合物通过动物的饮食，例如通过动物的固体饲料或饮用水来施用阳离子胆固醇添加剂。该方法包括向动物喂食由阳离子胆固醇添加剂（例如化合物与固醇骨架）和多个连接到其上的阳离子基团组成的饮食。饲料组合物可以包括固体或液体进料组分和阳离子胆固醇添加剂。这些方法和组合物可用于在限制饲料操作中饲养的动物，例如牛，猪，马，羊或家禽，并且可以减少消化道中的有害细菌，增加有益的细菌菌群，提高饲料转化效率，降低发病率 /或死亡率，和/或产生具有降低的有害细菌含量的收获肉。

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