-
公开(公告)号：US08592447B2
公开(公告)日：2013-11-26
申请号：US12312503
申请日：2007-11-13
Applicant: Michael K. Riscoe , Rolf Winter , Jane X. Kelly , David J. Hinrichs , Martin J. Smilkstein
Inventor： Michael K. Riscoe , Rolf Winter , Jane X. Kelly , David J. Hinrichs , Martin J. Smilkstein
IPC: A61K31/44 , C07D219/04
CPC classification number: C07D219/14 , A61K31/4706 , A61K31/473 , C07D219/06 , C07D401/06 , Y02A50/409 , Y02A50/411 , Y02A50/414 , Y02A50/423 , Y02A50/491
Abstract: A class of acridone compounds has been discovered that exhibits chemosensitizing and antiparasitic activity. Described herein are pharmaceutical compositions and methods for their use to treat parasitic infections, such as malaria and toxoplasmosis, and to sensitize resistant cells, such as multidrug resistant cells to other therapeutic agents. The pharmaceutical compositions and methods may also be used to treat and/or prevent psychotic diseases such as schizophrenia.
-
公开(公告)号：US20120115904A1
公开(公告)日：2012-05-10
申请号：US13153350
申请日：2011-06-03
Applicant: Michael K. Riscoe , Jane X. Kelly , Rolf W. Winter , David J. Hinrichs , Martin J. Smilkstein , Aaron Nilsen , Jeremy Burrows , Dennis Kyle , Roman Manetsch , Richard M. Cross , Andrii Monastyrskyi , David L. Flanigan
Inventor： Michael K. Riscoe , Jane X. Kelly , Rolf W. Winter , David J. Hinrichs , Martin J. Smilkstein , Aaron Nilsen , Jeremy Burrows , Dennis Kyle , Roman Manetsch , Richard M. Cross , Andrii Monastyrskyi , David L. Flanigan
CPC classification number: C07D215/233 , C07D215/42 , C07D215/60 , C07D239/90 , C07D279/16 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/06 , C07D413/04 , C07D491/052
Abstract: Compounds of formula I: or formula II: or a pharmaceutically acceptable salt of formula I or formula II, wherein: R1 is H, hydroxyl, alkoxy, acyl, alkyl, cycloalkyl, aryl, or heteroaryl; R2 is methyl or haloalkyl; R4 is hydroxyl, carbonyloxy, or carbonyldioxy; and R3 is aliphatic, aryl, aralkyl, or alkylaryl; and R5, R6, R7 and R8 are each individually H, halogen, alkoxy, alkyl, haloalkyl, aryl, nitro, cyano, amino, amido, acyl, carboxyl, substituted carboxyl, or —SO2R10, wherein R10 is H, alkyl, amino or haloalkyl; provided that in formula I, R5 and R are not both H or R6 is not H or methoxy; and in formula II that if R4 is carbonyldioxy then R7 is not methoxy.
Abstract translation: 式I化合物或式II化合物或式I或式II的药学上可接受的盐，其中：R 1是H，羟基，烷氧基，酰基，烷基，环烷基，芳基或杂芳基; R2是甲基或卤代烷基; R4是羟基，羰基氧基或羰基二氧基; 并且R 3是脂族，芳基，芳烷基或烷基芳基; 和R 5，R 6，R 7和R 8各自独立地为H，卤素，烷氧基，烷基，卤代烷基，芳基，硝基，氰基，氨基，酰胺基，酰基，羧基，取代的羧基或-SO 2 R 10，其中R 10为H，烷基，氨基 或卤代烷基; 条件是在式I中，R 5和R不同时为H或R 6不为H或甲氧基; 在式II中，如果R 4是羰基二氧基，那么R 7不是甲氧基。
-
公开(公告)号：US20120010237A1
公开(公告)日：2012-01-12
申请号：US13153347
申请日：2011-06-03
Applicant: Michael K. Riscoe , Jane X. Kelly , Rolf W. Winter , David J. Hinrichs , Martin J. Smilkstein , Aaron Nilsen
Inventor： Michael K. Riscoe , Jane X. Kelly , Rolf W. Winter , David J. Hinrichs , Martin J. Smilkstein , Aaron Nilsen
CPC classification number: C07D215/60 , C07D215/233 , C07D215/42 , C07D239/90 , C07D279/16 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/06 , C07D413/04 , C07D491/052
Abstract: A method for inhibiting a parasitic or infectious disease in a subject, wherein the parasitic or infectious disease is selected from one caused by Eimeria sp., Babesia sp., Theileria sp. or Neospora caninum, the method comprising administering to the subject a therapeutically effective amount of a compound of formula I: or formula II: or a pharmaceutically acceptable salt of formula I or formula II, wherein: R1 is H, hydroxyl, alkoxy, acyl, alkyl, cycloalkyl, aryl, or heteroaryl; R2 is methyl, haloalkyl, or heteroaryl; R4 is hydroxyl, carbonyloxy, or carbonyldioxy; R3 is aliphatic, aryl, aralkyl, or alkylaryl; and R5, R6, R7 and R8 are each individually H, halogen, alkoxy, alkyl, haloalkyl, aryl, nitro, cyano, amino, amido, acyl, carboxyl, substituted carboxyl, or —SO2R10, wherein R10 is H, alkyl, amino or haloalkyl; provided that in formula I, R5 and R7 are not H or R6 is not H or methoxy; and in formula II that if R4 is carbonyldioxy then R7 is not methoxy.
Abstract translation: 一种抑制受试者中寄生虫或感染性疾病的方法，其中寄生虫或感染性疾病选自艾美球虫（Eimeria sp。），巴贝虫属（Babesia sp。），The虫属 或新孢子虫（Neospora caninum），所述方法包括向受试者施用治疗有效量的式I或式II化合物或其药学上可接受的式I或式II的盐，其中：R 1是H，羟基，烷氧基，酰基， 烷基，环烷基，芳基或杂芳基; R2是甲基，卤代烷基或杂芳基; R4是羟基，羰基氧基或羰基二氧基; R3是脂族，芳基，芳烷基或烷基芳基; 和R 5，R 6，R 7和R 8各自独立地为H，卤素，烷氧基，烷基，卤代烷基，芳基，硝基，氰基，氨基，酰胺基，酰基，羧基，取代的羧基或-SO 2 R 10，其中R 10为H，烷基，氨基 或卤代烷基; 条件是在式I中，R 5和R 7不是H或R 6不是H或甲氧基; 在式II中，如果R 4是羰基二氧基，那么R 7不是甲氧基。
-
Patent Agency Ranking
公开(公告)号：US08598354B2
公开(公告)日：2013-12-03
申请号：US13153350
申请日：2011-06-03
Applicant: Michael K. Riscoe , Jane X. Kelly , Rolf W. Winter , David J. Hinrichs , Martin J. Smilkstein , Aaron Nilsen , Jeremy Burrows , Dennis Kyle , Roman Manetsch , Richard M. Cross , Andrii Monastyrskyi , David L. Flanigan
Inventor： Michael K. Riscoe , Jane X. Kelly , Rolf W. Winter , David J. Hinrichs , Martin J. Smilkstein , Aaron Nilsen , Jeremy Burrows , Dennis Kyle , Roman Manetsch , Richard M. Cross , Andrii Monastyrskyi , David L. Flanigan
CPC classification number: C07D215/233 , C07D215/42 , C07D215/60 , C07D239/90 , C07D279/16 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/06 , C07D413/04 , C07D491/052
Abstract: Compounds of formula I: or formula II: or a pharmaceutically acceptable salt of formula I or formula II, wherein: R1 is H, hydroxyl, alkoxy, acyl, alkyl, cycloalkyl, aryl, or heteroaryl; R2 is methyl or haloalkyl; R4 is hydroxyl, carbonyloxy, or carbonyldioxy; and R3 is aliphatic, aryl, aralkyl, or alkylaryl; and R5, R6, R7 and R8 are each individually H, halogen, alkoxy, alkyl, haloalkyl, aryl, nitro, cyano, amino, amido, acyl, carboxyl, substituted carboxyl, or —SO2R10, wherein R10 is H, alkyl, amino or haloalkyl; provided that in formula I, R5 and R7 are not both H or R6 is not H or methoxy; and in formula II that if R4 is carbonyldioxy then R7 is not methoxy.
Abstract translation: 式I化合物或式II化合物或式I或式II的药学上可接受的盐，其中：R 1是H，羟基，烷氧基，酰基，烷基，环烷基，芳基或杂芳基; R2是甲基或卤代烷基; R4是羟基，羰基氧基或羰基二氧基; 并且R 3是脂族，芳基，芳烷基或烷基芳基; 和R 5，R 6，R 7和R 8各自独立地为H，卤素，烷氧基，烷基，卤代烷基，芳基，硝基，氰基，氨基，酰胺基，酰基，羧基，取代的羧基或-SO 2 R 10，其中R 10为H，烷基，氨基 或卤代烷基; 条件是在式Ⅰ中，R5和R7不同时为H或R6不为H或甲氧基; 在式II中，如果R 4是羰基二氧基，那么R 7不是甲氧基。
-
5.发明申请INACTIVE ISOMER COMPOSITIONS FOR USE AS DRUG-RESISTANCE-REVERSAL AGENTS AND IN PROPHYLACTIC TREATMENT 审中-公开用作抗药性反转剂和预防治疗的不活动异构体组合物公开(公告)号：US20080194652A1
公开(公告)日：2008-08-14
申请号：US12104267
申请日：2008-04-16
Applicant: Martin J. Smilkstein
Inventor： Martin J. Smilkstein
IPC: A61K31/4402 , A61P37/08
CPC classification number: A61K31/137 , A61K31/4172 , A61K31/495 , Y02A50/411
Abstract: A method of using inactive isomer compositions as drug-resistance-reversal agents and in prophylactic treatment includes the steps of selecting an antihistaminically-inactive isomer of a preselected antihistamine, and making stereoselective use of the antihistaminically-inactive isomer for a clinical purposes. The making step includes choosing one of the following clinical purposes for which to make stereoselective use of the antihistaminically-inactive isomer: treatment of malaria, prophylaxis of malaria; and treatment of drug-resistant malignancies. The step of selecting an antihistaminically-inactive isomer involves preselecting an antihistamine from the group consisting of chlorpheniramine (−), brompheniramine (−), fluorpheniramine (−), pheniramine (−), bromodiphenhydramine, doxylamine, prophenpyridamine, chlorcyclizine, dimethindene (+), carbinoxamine (+), chlorphenoxamine, clemastine, orphenadrine, hydroxyzine, meclizine, and buclizine. Various inactive isomer compositions are disclosed for the above-described clinical purposes.
Abstract translation: 使用无活性异构体组合物作为药物抗性逆转剂和预防性治疗的方法包括选择预选的抗组胺药的抗组胺活性异构体的步骤，并为了临床目的使立体选择性使用抗组胺活性异构体。 制备步骤包括选择以下用于立体选择性使用抗组胺活性异构体的临床目的之一：治疗疟疾，预防疟疾; 和治疗耐药性恶性肿瘤。 选择抗组胺活性异构体的步骤包括从组合氯苯那敏（ - ），溴苯那敏（ - ），氟苯那敏（ - ），苯吡胺（ - ），溴代苯海拉明，多西拉敏，丙烯吡啶胺，氯氰菊酯，二甲基茚（+） ，卡非那敏（+），氯苯氧胺，克立姆斯他汀，奥芬那君，羟嗪，麦地利和大疱。 为了上述临床目的，公开了各种惰性异构体组合物。
-
公开(公告)号：US07829578B1
公开(公告)日：2010-11-09
申请号：US11633509
申请日：2006-12-05
Applicant: Michael K. Riscoe , Rolf W. Winter , Jane X. Kelly , Martin J. Smilkstein , David J. Hinrichs
Inventor： Michael K. Riscoe , Rolf W. Winter , Jane X. Kelly , Martin J. Smilkstein , David J. Hinrichs
IPC: C07D215/38 , A61K31/04
CPC classification number: A61K31/4706 , A61K31/04 , A61K31/44 , A61K45/06 , C07D213/68 , C07D215/233 , C07D221/08 , C07D311/86 , Y02A50/411 , A61K2300/00
Abstract: Aromatic ketones having an extended fluoro-alkyl or fluoro-alkoxy moiety are disclosed. In particular aspects, the compounds comprise substituted 9-acridone, 9-xanthone, 4(1H)-quinolone, 4(1H) pyridone, 1,4-naphthoquinone, 9,10-anthraquinone derivatives. These preparations possess potent pharmacological activity for inhibiting malaria and mosquito-borne (Plasmodium) diseases. The haloalkyl/alkoxy aromatic compounds possess significant pharmacological activity, with IC50 values in the nanomolar and sub-nanomolar range, and reduced toxicity against host derived cells and tissues. Methods of using the fluoro-alkyl/alkoxy aromatic compounds in the treatment of malaria and other human and animal diseases are also disclosed. Agricultural uses of the fluoro-alkyl/alkoxy aromatic compounds, such as in control of fungal diseases and in the production of important commercial crops (apples, etc.), are also presented.
Abstract translation: 公开了具有延伸的氟烷基或氟 - 烷氧基部分的芳族酮。 在特定方面，化合物包括取代的9-吖啶酮，9-呫吨酮，4（1H） - 喹诺酮，4（1H）吡啶酮，1,4-萘醌，9,10-蒽醌衍生物。 这些制剂具有有效的药理活性，可用于抑制疟疾和蚊子（疟原虫）疾病。 卤代烷基/烷氧基芳族化合物具有显着的药理活性，IC50值在纳摩尔和亚纳摩尔范围内，对宿主衍生的细胞和组织的毒性降低。 还公开了使用氟 - 烷基/烷氧基芳族化合物治疗疟疾和其他人和动物疾病的方法。 还介绍了氟 - 烷基/烷氧基芳族化合物的农业用途，如控制真菌病和重要的商业作物（苹果等）的生产。
-
公开(公告)号：US20100069428A1
公开(公告)日：2010-03-18
申请号：US12312503
申请日：2007-11-13
Applicant: Michael K. Riscoe , Rolf Winter , Jane X. Kelly , David J. Hinrichs , Martin J. Smilkstein
Inventor： Michael K. Riscoe , Rolf Winter , Jane X. Kelly , David J. Hinrichs , Martin J. Smilkstein
IPC: A61K31/473 , C07D219/06 , A61P33/06
CPC classification number: C07D219/14 , A61K31/4706 , A61K31/473 , C07D219/06 , C07D401/06 , Y02A50/409 , Y02A50/411 , Y02A50/414 , Y02A50/423 , Y02A50/491
Abstract: A class of acridone compounds has been discovered that exhibits chemosensitizing and antiparasitic activity. Described herein are pharmaceutical compositions and methods for their use to treat parasitic infections, such as malaria and toxoplasmosis, and to sensitize resistant cells, such as multidrug resistant cells to other therapeutic agents. The pharmaceutical compositions and methods may also be used to treat and/or prevent psychotic diseases such as schizophrenia.
Abstract translation: 已经发现一类具有化学敏感性和抗寄生虫活性的吖啶酮化合物。 本文描述了用于治疗寄生虫感染如疟疾和弓形虫病的药物组合物和方法，并使抗药性细胞（例如多药耐药性细胞）对其它治疗剂敏感。 药物组合物和方法也可用于治疗和/或预防精神病如精神分裂症。
-
公开(公告)号：US20080108655A1
公开(公告)日：2008-05-08
申请号：US11352388
申请日：2006-02-10
Applicant: Martin J. Smilkstein
Inventor： Martin J. Smilkstein
IPC: A61K31/135 , A61K31/47 , A61P33/06 , A61P35/00
CPC classification number: A61K31/4706 , Y02A50/411
Abstract: A method of treating a malarial infection includes using orphenadrine as part of treating the infection. The method may use orphenadrine alone or in combination with another antimalarial drug, such as chloroquine, or with plural antimalarial drugs. Use of orphenadrine in this way may also be used in a method of providing prophylaxis against a malarial infection, and as part of a method of treating a malignancy.
Abstract translation: 治疗疟疾感染的方法包括使用奥芬那君作为治疗感染的一部分。 该方法可以单独或与另一种抗疟疾药物如氯喹或多种抗疟药物组合使用奥芬那普。 以这种方式使用奥芬那君也可以用于提供针对疟疾感染的预防的方法，以及作为治疗恶性肿瘤的方法的一部分。
-
-
-
-
-
-
-
Search Results
8
records
(took 0.012 seconds)
