公开(公告)号：US20030181495A1

公开(公告)日：2003-09-25

申请号：US10394794

申请日：2003-03-21

申请人： Medinox, Inc.

发明人： Ching-San Lai ,  Vassil P. Vassilev

IPC分类号： A61K031/426 ,  A61K031/325 ,  A61K031/55 ,  A61K031/4545 ,  A61K031/4025

CPC分类号： A61K45/06 ,  A61K31/145 ,  A61K31/4025 ,  A61K31/4545 ,  A61K31/5377 ,  Y02A50/411

摘要： The present invention provides novel combinations of dithiocarbamate disulfide dimers with other active agents. In one method, the disulfide derivative of a dithiocarbamate is coadministered with a thiazolidinedione for the treatment of diabetes. In another embodiment, In another embodiment, invention combinations further comprise additional active agents such as, for example, metformin, insulin, sulfonylureas, and the like. In another embodiment, the present invention relates to compositions and formulations useful in such therapeutic methods.

摘要翻译： 本发明提供二硫代氨基甲酸酯二硫化物二聚体与其它活性剂的新颖组合。 在一种方法中，二硫代氨基甲酸二硫化物衍生物与噻唑烷二酮共同给药以治疗糖尿病。 在另一个实施方案中，在另一个实施方案中，本发明组合还包含另外的活性剂，例如二甲双胍，胰岛素，磺酰脲等。 在另一个实施方案中，本发明涉及可用于这种治疗方法的组合物和制剂。

公开(公告)号：US20140350097A1

公开(公告)日：2014-11-27

申请号：US13901323

申请日：2013-05-23

申请人： Medinox,Inc.

发明人： Ching-San Lai

IPC分类号： A61K31/27 ,  G01N33/50 ,  A61K31/165

CPC分类号： A61K31/27 ,  A61K31/165 ,  A61K31/28 ,  A61K33/26 ,  G01N33/50 ,  G01N33/84 ,  G01N2333/90254 ,  G01N2800/52 ,  Y10T436/173076 ,  Y10T436/177692 ,  A61K2300/00

摘要： There is provided a method for the prevention and/or treatment of hypotension associated with hemodialysis, which method includes administering to a subject in need thereof an effective amount of at least one physiologically compatible compound which, in combination with iron, binds nitric oxide. There is further provided a method for identifying hemodialysis subjects for whom treatment with an effective amount of at least one physiologically compatible compound which, in combination with iron, binds nitric oxide is indicated. The method includes monitoring the subject's nitric oxide levels, and selecting those subjects having elevated nitric oxide levels for treatment with an effective amount of at least one physiologically compatible compound which, in combination with iron, binds nitric oxide, wherein the effective amount is sufficient to maintain the subject's nitric oxide levels within an acceptable range.

摘要翻译： 提供了用于预防和/或治疗与血液透析相关的低血压的方法，该方法包括向有需要的受试者施用有效量的与铁结合的至少一种生理上相容的化合物结合一氧化氮。 还提供了一种用于鉴定血液透析受试者的方法，用有效量的至少一种与铁结合一氧化氮的生理相容性化合物进行治疗。 该方法包括监测受试者的一氧化氮水平，并选择具有升高的一氧化氮水平的受试者用有效量的至少一种生理上相容的化合物进行治疗，所述化合物与铁结合一氧化氮，其中有效量足以 将受试者的一氧化氮水平维持在可接受的范围内。

公开(公告)号：US20030220468A1

公开(公告)日：2003-11-27

申请号：US10434371

申请日：2003-05-07

申请人： Medinox, Inc.

发明人： Ching-San Lai ,  Tingmin Wang

IPC分类号： C07K005/04 ,  C07C317/22

CPC分类号： A61K47/555 ,  A61K47/54 ,  A61K47/545

摘要： In accordance with the present invention, there are provided modified forms of nonsteroidal anti-inflamamatory drugs (NSAIDs). Modified NSAIDs according to the invention provide a new class of anti-inflammatory agent which provide the therapeutic benefits of NSAIDs while causing a much lower incidence of side-effects then typically observed with such agents.

摘要翻译： 根据本发明，提供了非甾体抗炎症药物（NSAID）的修饰形式。 根据本发明的修饰的NSAID提供了一类新的抗炎剂，其提供NSAIDs的治疗益处，同时引起副作用的发生率低得多，然后通常用这些药剂观察到。

公开(公告)号：US20030087840A1

公开(公告)日：2003-05-08

申请号：US10176396

申请日：2002-06-18

申请人： Medinox, Inc.

发明人： Ching-San Lai ,  Tingmin Wang

IPC分类号： A61K031/7008 ,  A61K031/66 ,  A61K031/401 ,  A61K031/325

CPC分类号： A61K31/7008 ,  A61K31/325 ,  A61K31/401 ,  A61K31/66 ,  A61K47/555

摘要： In accordance with the present invention, there are provided conjugates of nitric oxide scavengers (e.g., dithiocarbamates, or nullDCnull) and pharmacologically active agents (e.g., NSAIDs). Invention conjugates provide a new class of pharmacologically active agents (e.g., anti-inflammatory agents) which cause a much lower incidence of side-effects due to the protective effects imparted by modifying the pharmacologically active agents as described herein. In addition, invention conjugates are more effective than unmodified pharmacologically active agents because cells and tissues contacted by the pharmacologically active agent(s) are protected from the potentially damaging effects of nitric oxide overproduction induced thereby as a result of the co-production of nitric oxide scavenger (e.g., dithiocarbamate), in addition to free pharmacologically active agent, when invention conjugate is cleaved.

公开(公告)号：US20040077691A1

公开(公告)日：2004-04-22

申请号：US10277998

申请日：2002-10-21

申请人： Medinox, Inc.

发明人： Tingmin Wang ,  Ching-San Lai

IPC分类号： A61K031/44 ,  A61K031/401 ,  A61K031/325

CPC分类号： C07D253/08 ,  A61K31/425 ,  A61K31/53 ,  C07C259/06 ,  C07C259/10 ,  C07C271/08 ,  C07C311/48 ,  C07C317/44 ,  C07C323/60 ,  C07D209/28 ,  C07D277/36

摘要： In accordance with the present invention, there are provided novel chemical entities which have multiple utilities, e.g., as prodrugs of NSAIDs; as dual inhibitors of cyclooxygenase (COX) and 5-lipoxygenase (5-LO); as anticancer agents (through promoting apoptosis and/or inhibiting the matrix metalloproteinases (MMPs)); as anti-diabetics; and the like. Invention compounds comprise a non-steroidal anti-inflammatory agent (NSAID), covalently linked to a hydroxamate. Invention compounds are useful alone or in combination with one or more additional pharmacologically active agents, and can be used for a variety of applications, such as, for example, treating inflammation and inflammation-related conditions; reducing the side effects associated with administration of anti-inflammatory agents; promoting apoptosis; inhibiting matrix metalloproteinases; as anti-diabetic agents; and the like.

摘要翻译： 根据本发明，提供了具有多种用途的新型化学实体，例如作为NSAID的前药; 作为环氧合酶（COX）和5-脂氧合酶（5-LO）的双重抑制剂; 作为抗癌剂（通过促进细胞凋亡和/或抑制基质金属蛋白酶（MMPs））; 作为抗糖尿病患者; 等等。 本发明化合物包含与羟肟酸共价连接的非甾体抗炎剂（NSAID）。 本发明化合物可单独使用或与一种或多种另外的药理学活性剂组合使用，并且可用于多种应用，例如治疗炎症和炎症相关病症; 减少与抗炎剂的施用相关的副作用; 促进凋亡; 抑制基质金属蛋白酶; 作为抗糖尿病药; 等等。

公开(公告)号：US20030149021A1

公开(公告)日：2003-08-07

申请号：US10157733

申请日：2002-05-28

申请人： Medinox, Inc.

发明人： Runtao Li ,  Tieming Cheng ,  Jingrong Cui ,  Tingmin Wang

IPC分类号： C07D279/12 ,  C07D265/32 ,  A61K031/55 ,  A61K031/553 ,  A61K031/554 ,  A61K031/551 ,  A61K031/54 ,  A61K031/537 ,  A61K031/495

CPC分类号： C07D215/22

摘要： In accordance with the present invention, there is provided a new class of compounds, i.e., mono(dithio)carbamate esters of piperazine and analogs thereof, with or without substituents. Also provided are methods for the preparation of invention compounds and the pharmaceutical use thereof in the treatment of a variety of pathological conditions, especially for the treatment of cancers. A lead compound has shown good anticancer activity with low toxicity.

摘要翻译： 根据本发明，提供了一类新的化合物，即具有或不具有取代基的哌嗪及其类似物的单（二硫代）氨基甲酸酯。 还提供了用于制备本发明化合物的方法及其药物用途，用于治疗各种病理状况，特别是用于治疗癌症。 铅化合物具有良好的抗癌活性，毒性低。

公开(公告)号：US20030088111A1

公开(公告)日：2003-05-08

申请号：US10097197

申请日：2002-03-12

申请人： Medinox, Inc.

发明人： Ching-San Lai ,  Tingmin Wang

IPC分类号： C07D209/18 ,  C07C39/70

CPC分类号： A61K47/555 ,  A61K47/54

摘要： In accordance with the present invention, there are provided normal modified forms of nonsteroidal anti-inflamamatory drugs. Modified NSAIDs according to the invention provide a new class of anti-inflammatory agent which provide the therapeutic benefits of NSAIDs while causing a much lower incidence of side-effects then typically observed with such agents.

摘要翻译： 根据本发明，提供了非甾体抗炎药的正常修饰形式。 根据本发明的修饰的NSAID提供了一类新的抗炎剂，其提供NSAIDs的治疗益处，同时引起副作用的发生率低得多，然后通常用这些药剂观察到。

公开(公告)号：US20030022923A1

公开(公告)日：2003-01-30

申请号：US10097173

申请日：2002-03-12

申请人： Medinox, Inc.

发明人： Ching-San Lai ,  Vassil P. Vassilev ,  Long-Shiuh Chen

IPC分类号： A61K031/426 ,  A61K031/335 ,  A61K031/13 ,  A61K031/11

CPC分类号： A61K45/06 ,  A61K31/11 ,  A61K31/13 ,  A61K31/335 ,  A61K31/426 ,  A61K33/30 ,  A61K2300/00

摘要： The preparation and use of a protected organic aldehyde is described wherein bioavailability of the orally administered therapeutic aldehyde is improved. The protected aldehyde is prepared by reacting the aldehyde with a protecting group, for example, condensing the aldehyde chemically with a thiazolidine-4-carboxylic acid. The improved bioavailability of such orally administered drugs increases the feasibility of delivering sufficient amounts of vanillin or other therapeutic organic aldehydes in vivo to prevent sickling in sickle cell anemia. Combination therapy is also described wherein a protected organic aldehyde is administered to a subject in treatment of sickle cell anemia in conjunction with one or more other drugs, such as pain killers, used in treatment of the symptoms of sickle cell anemia or sickle cell disease.

公开(公告)号：US20020151540A1

公开(公告)日：2002-10-17

申请号：US10044096

申请日：2002-01-11

申请人： Medinox, Inc.

发明人： Ching-San Lai ,  Vassil Vassilev

IPC分类号： A61K031/55 ,  A61K031/4545 ,  A61K031/4025 ,  A61K031/325

CPC分类号： A61K31/4025 ,  A61K31/4545 ,  Y02A50/409 ,  Y02A50/411 ,  Y02A50/423 ,  Y10S514/851

摘要： The present invention provides a novel dithiocarbamamte disulfide dimer useful in various therapeutic treatments, either alone or in combination with other active agents. In one method, the disulfide derivative of a dithiocarbamate is coadministered with an agent that inactivates (or inhibits the production of) species that induce the expression of nitric oxide synthase to reduce the production of such species, while, at the same time reducing nitric oxide levels in the subject. In another embodiment, free iron ion levels are reduced in a subject by administration of a disulfide derivative of a dithiocarbamate(s) to scavenge free iron ions, for example, in subjects undergoing anthracycline chemotherapy. In another embodiment, cyanide levels are reduced in a subject by administration of a disulfide derivative of a dithiocarbamate so as to bind cyanide in the subject. In a further aspect, the present invention relates to compositions and formulations useful in such therapeutic methods.

摘要翻译： 本发明提供了可用于各种治疗处理的新型二硫代氨基甲酰二硫化物二聚体，单独或与其它活性剂组合。 在一种方法中，二硫代氨基甲酸二硫化物衍生物与灭活（或抑制产生）诱导一氧化氮合成酶表达的物质共同施用，以减少这种物质的产生，同时还原一氧化氮 主题级别。 在另一个实施方案中，通过给予二硫代氨基甲酸二硫化物衍生物来清除游离铁离子，例如在接受蒽环类化疗的受试者中游离铁离子水平降低。 在另一个实施方案中，通过施用二硫代氨基甲酸盐的二硫化物衍生物以使受试者中的氰化物结合，在受试者中氰化物水平降低。 在另一方面，本发明涉及可用于这种治疗方法的组合物和制剂。