公开(公告)号：US08435971B2

公开(公告)日：2013-05-07

申请号：US13169781

申请日：2011-06-27

申请人： Pedro Cuevas Sánchez ,  Antonio Romero Garrido ,  Guillermo Gimenez Gallego ,  Serafin Valverde Lopez ,  Rosa Maria Lozano Puerto

发明人： Pedro Cuevas Sánchez ,  Antonio Romero Garrido ,  Guillermo Gimenez Gallego ,  Serafin Valverde Lopez ,  Rosa Maria Lozano Puerto

IPC分类号： A61K31/185 ,  A61K31/56 ,  A01N37/00 ,  A01N45/00

CPC分类号： A61K31/185

摘要： The invention relates to the use of 2,5-dihydroxybenzenesulfonic acid in the production of medicaments for the treatment of angiodependent diseases. More specifically, the invention relates to the use of the aforesaid compound and, in particular, the calcium and potassium salts thereof, for the treatment of two angiodependent diseases, which present a reduction in the apoptosis, namely cancer and psoriasis. The invention also discloses the antiproliferative, antimigratory, antiangiogenic and proapoptotic capacity of said family of compounds in non-quiescent cells. In addition, the invention details the potentiating effect of said compounds on known cytostatic medicines in the treatment of tumours and, specifically, on gliomas. The invention further relates to the therapeutic efficacy of said compounds, based on the combined antiproliferative, antiangiogenic and proapaptotic capacities thereof, in the treatment of chronic psoriatic plaques.

摘要翻译： 本发明涉及2,5-二羟基苯磺酸在制备用于治疗依赖性疾病的药物中的用途。 更具体地，本发明涉及上述化合物，特别是其钙和钾盐用于治疗呈现细胞凋亡降低（即癌症和牛皮癣）的两种血液依赖性疾病的用途。 本发明还公开了所述家族化合物在非静止细胞中的抗增殖，抗微生物，抗血管生成和促凋亡能力。 此外，本发明详细描述了所述化合物对已知的细胞生长抑制药物在治疗肿瘤中，特别是胶质瘤的增强作用。 本发明进一步涉及所述化合物在治疗慢性银屑病斑块的基础上结合抗增生性，抗血管生成和促血细胞生成能力的治疗功效。

公开(公告)号：US20080293816A1

公开(公告)日：2008-11-27

申请号：US10588166

申请日：2005-02-16

申请人： Pedro Cuevas Sanchez ,  Antonio Romero Garrido ,  Guillermo Gimenez Gallego ,  Serafin Valverde Lopez ,  Rosa Maria Lozano Puerto

发明人： Pedro Cuevas Sanchez ,  Antonio Romero Garrido ,  Guillermo Gimenez Gallego ,  Serafin Valverde Lopez ,  Rosa Maria Lozano Puerto

IPC分类号： A61K31/185 ,  C07C309/29 ,  A61P35/00 ,  A61P17/06

CPC分类号： A61K31/185

摘要： The invention relates to the use of 2,5-dihydroxybenzenesulfonic acid in the production of medicaments for the treatment of angiodependent diseases. More specifically, the invention relates to the use of the aforesaid compound and, in particular, the calcium and potassium salts thereof, for the treatment of two angiodependent diseases, which present a reduction in the apoptosis, namely cancer and psoriasis. The invention also discloses the antiproliferative, antimigratory, antiangiogenic and proapoptotic capacity of said family of compounds in non-quiescent cells. In addition, the invention details the potentiating effect of said compounds on known cytostatic medicines in the treatment of tumours and, specifically, on gliomas. The invention further relates to the therapeutic efficacy of said compounds, based on the combined antiproliferative, antiangiogenic and proapoptotic capacities thereof, in the treatment of chronic psoriatic plaques.

摘要翻译： 本发明涉及2,5-二羟基苯磺酸在制备用于治疗依赖性疾病的药物中的用途。 更具体地，本发明涉及上述化合物，特别是其钙和钾盐用于治疗呈现细胞凋亡降低（即癌症和牛皮癣）的两种血液依赖性疾病的用途。 本发明还公开了所述家族化合物在非静止细胞中的抗增殖，抗微生物，抗血管生成和促凋亡能力。 此外，本发明详细描述了所述化合物对已知的细胞生长抑制药物在治疗肿瘤中，特别是胶质瘤的增强作用。 本发明进一步涉及所述化合物在治疗慢性银屑病斑块的基础上结合抗增殖，抗血管生成和促凋亡能力的治疗功效。

公开(公告)号：US20090111779A1

公开(公告)日：2009-04-30

申请号：US12257854

申请日：2008-10-24

申请人： Pedro Cuevas Sanchez ,  Antonio Romero Garrido ,  Guillermo Gimenez Gallego ,  Serafin Valverde Lopez ,  Rosa Maria Lozano Puerto

发明人： Pedro Cuevas Sanchez ,  Antonio Romero Garrido ,  Guillermo Gimenez Gallego ,  Serafin Valverde Lopez ,  Rosa Maria Lozano Puerto

IPC分类号： A61K31/59 ,  A61K31/185 ,  A61K31/192 ,  A61K31/56 ,  A61P35/00 ,  A61P17/00

CPC分类号： A61K31/185 ,  A61K9/0014 ,  A61K31/095 ,  A61K31/56 ,  A61K31/59 ,  A61K31/60 ,  A61K45/06 ,  C07C309/29

摘要： The invention describes compositions and methods of use for 2,5-dihydroxybenzene sulfonic acid compounds and pharmaceutically acceptable salts thereof. The invention provides methods for (a) treating skin cancer; (b) treating cancer of the organs; (c) treating leukemia; (d) improving the efficacy of chemotherapy, radiation therapy and/or cancer immunotherapy; (e) treating rosacea; and (f) treating psoriasis by administration of a composition comprising at least one 2,5-dihydroxybenzene sulfonic acid compound or a pharmaceutically acceptable salt thereof, and, optionally at least one therapeutic agent. Also disclosed are compositions comprising administration of at least one 2,5-dihydroxybenzene sulfonic acid compound, or a pharmaceutically acceptable salt thereof, and, at least one therapeutic agent. In the invention the 2,5-dihydroxybenzene sulfonic acid compounds or pharmaceutically acceptable salts thereof are 2,5-dihydroxybenzene sulfonic acid, calcium 2,5-dihydroxybenzenesulfonate, potassium 2,5-dihydroxybenzenesulfonate, magnesium 2,5-dihydroxybenzenesulfonate and diethylamine 2,5-dihydroxybenzenesulfonate.

摘要翻译： 本发明描述了用于2,5-二羟基苯磺酸化合物的组合物和方法及其药学上可接受的盐。 本发明提供（a）治疗皮肤癌的方法; （b）治疗器官的癌症; （c）治疗白血病; （d）提高化疗，放射治疗和/或癌症免疫治疗的疗效; （e）治疗酒渣鼻; 和（f）通过施用包含至少一种2,5-二羟基苯磺酸化合物或其药学上可接受的盐的组合物和任选的至少一种治疗剂来治疗牛皮癣。 还公开了包含施用至少一种2,5-二羟基苯磺酸化合物或其药学上可接受的盐和至少一种治疗剂的组合物。 在本发明中，2,5-二羟基苯磺酸化合物或其药学上可接受的盐是2,5-二羟基苯磺酸，2,5-二羟基苯磺酸钙，2,5-二羟基苯磺酸钾，2,5-二羟基苯磺酸镁和二乙胺2， 5-二羟基苯磺酸盐。

公开(公告)号：US20090076140A1

公开(公告)日：2009-03-19

申请号：US12264000

申请日：2008-11-03

申请人： Beatriz Maria Banfi Tosi ,  Guillermo Gimenez Gallego ,  Serafin Valverde Lopez ,  Rosa Maria Lozano Puerto ,  Pedro Sanchez Cuevas

发明人： Beatriz Maria Banfi Tosi ,  Guillermo Gimenez Gallego ,  Serafin Valverde Lopez ,  Rosa Maria Lozano Puerto ,  Pedro Sanchez Cuevas

IPC分类号： A61K31/255 ,  A61P19/02 ,  A61P17/06 ,  A61P3/04 ,  A61P9/10

CPC分类号： A61K31/47 ,  A61K31/185

摘要： A naphthalenesulfonic acid or quinolinesulfonic acid of formula (I), wherein A is N or a CR8 formula group, where R8 is H, OH, NR10OR11, independently from one another, where R10 and R11 represent H or C1-C6 alkyl or a group of formula NH—CO—R12, where R12 is C1-C6 alkyl or C6-C10 aryl; R1 and R2 represent H or SO3R9, independently from one another, where R9 is H, ammonium or a cation of an alkali or alkaline-earth metal; R3 is H or OH; and R4, R5, R6 and R7 represent H, an NR10R11 or NH—CO—R12 group, independently from one another; on the condition that (i) at least one of R1 or R2 is SO3R9, and (ii) at least one of R4, R5, R6 or R7 is an NR10R11 or NH—CO—R12 group, or their pharmaceutically acceptable salts; and a pharmaceutically acceptable excipient.

摘要翻译： 式（I）的萘磺酸或喹啉磺酸，其中A为N或CR 8式基团，其中R 8为H，OH，NR 10 OR 11，彼此独立地为R 10和R 11表示H或C 1 -C 6烷基或基团 式NH-CO-R12，其中R12是C1-C6烷基或C6-C10芳基; R1和R2彼此独立地表示H或SO3R9，其中R9是H，铵或碱金属或碱土金属的阳离子; R3为H或OH; R4，R5，R6和R7彼此独立地表示H，NR10R11或NH-CO-R12基团; 在（i）R 1或R 2中的至少一个为SO 3 R 9的情况下，和（ii）R 4，R 5，R 6或R 7中的至少一个为NR 10 R 11或NH-CO-R 12基团或其药学上可接受的盐; 和药学上可接受的赋形剂。

公开(公告)号：US20070149618A1

公开(公告)日：2007-06-28

申请号：US11506469

申请日：2006-08-16

申请人： Pedro Cuevas Sanchez ,  Antonio Romero Garrido ,  Guillermo Gimenez Gallego ,  Serafin Valverde Lopez ,  Rosa Lozano Puerto

发明人： Pedro Cuevas Sanchez ,  Antonio Romero Garrido ,  Guillermo Gimenez Gallego ,  Serafin Valverde Lopez ,  Rosa Lozano Puerto

IPC分类号： A61K31/185 ,  A61K31/60 ,  A61K31/59 ,  A61K31/56

CPC分类号： A61K31/185 ,  A61K9/0014 ,  A61K31/095 ,  A61K31/56 ,  A61K31/59 ,  A61K31/60 ,  A61K45/06 ,  C07C309/29

摘要： The invention describes compositions and methods of use for 2,5-dihydroxybenzene sulfonic acid compounds and pharmaceutically acceptable salts thereof. The invention provides methods for (a) treating skin cancer; (b) treating cancer of the organs; (c) treating leukemia; (d) improving the efficacy of chemotherapy, radiation therapy and/or cancer immunotherapy; (e) treating rosacea; and (f) treating psoriasis by administration of a composition comprising at least one 2,5-dihydroxybenzene sulfonic acid compound or a pharmaceutically acceptable salt thereof, and, optionally at least one therapeutic agent. Also disclosed are compositions comprising administration of at least one 2,5-dihydroxybenzene sulfonic acid compound, or a pharmaceutically acceptable salt thereof, and, at least one therapeutic agent. In the invention the 2,5-dihydroxybenzene sulfonic acid compounds or pharmaceutically acceptable salts thereof are 2,5-dihydroxybenzene sulfonic acid, calcium 2,5-dihydroxybenzenesulfonate, potassium 2,5-dihydroxybenzenesulfonate, magnesium 2,5-dihydroxybenzenesulfonate and diethylamine 2,5-dihydroxybenzenesulfonate.

摘要翻译： 本发明描述了用于2,5-二羟基苯磺酸化合物的组合物和方法及其药学上可接受的盐。 本发明提供（a）治疗皮肤癌的方法; （b）治疗器官的癌症; （c）治疗白血病; （d）提高化疗，放射治疗和/或癌症免疫治疗的疗效; （e）治疗酒渣鼻; 和（f）通过施用包含至少一种2,5-二羟基苯磺酸化合物或其药学上可接受的盐的组合物和任选的至少一种治疗剂来治疗牛皮癣。 还公开了包含施用至少一种2,5-二羟基苯磺酸化合物或其药学上可接受的盐和至少一种治疗剂的组合物。 在本发明中，2,5-二羟基苯磺酸化合物或其药学上可接受的盐是2,5-二羟基苯磺酸，2,5-二羟基苯磺酸钙，2,5-二羟基苯磺酸钾，2,5-二羟基苯磺酸镁和二乙胺2， 5-二羟基苯磺酸盐。

公开(公告)号：US20060160849A1

公开(公告)日：2006-07-20

申请号：US10549221

申请日：2004-03-05

申请人： Beatriz Banfi Tosi ,  Guillermo Gimenez Gallego ,  Serafin Valverde Lopez ,  Rosa Lozano Puerto ,  Pedro Sanchez Cuevas

发明人： Beatriz Banfi Tosi ,  Guillermo Gimenez Gallego ,  Serafin Valverde Lopez ,  Rosa Lozano Puerto ,  Pedro Sanchez Cuevas

IPC分类号： A61K31/47 ,  A61K31/185

CPC分类号： A61K31/47 ,  A61K31/185

摘要： A naphthalenesulfonic acid or quinolinesulfonic acid of formula (I), wherein A is N or a CR8 formula group, where R8 is H, OH, NR10R11, independently from one another, where R10 and R11 represent H or C1-C6 alkyl or a group of formula NH—CO—R12, where R12 is C1-C6 alkyl or C6-C10 aryl; R1 and R2 represent H or SO3R9, independently from one another, where R9 is H, ammonium or a cation of an alkali or alkaline-earth metal; R3 is H or OH; and R4, R5, R6 and R7 represent H, an NR10R11 or NH—CO—R12 group, independently from one another; on the condition that (i) at least one of R1 or R2 is SO3R9, and (ii) at least one of R4, R5, R6 or R7 is an NR10R11 or NH—CO—R12 group, or their pharmaceutically acceptable salts; and a pharmaceutically acceptable excipient.

摘要翻译： 式（I）的萘磺酸或喹啉磺酸，其中A为N或CR 8式基团，其中R 8为H，OH，NR 10 其中R 10和R 11彼此独立地表示H或C 1 ，其中R 10和R 11独立地表示H或C 1 其中R 12是C 1 -C 12烷基或式NH-CO-R 12基团，其中R 12是C 1〜 -C 6 -C 6烷基或C 6 -C 10芳基; R 1和R 2彼此独立地表示H或SO 3 R 9，其中R > 9是H，铵或碱金属或碱土金属的阳离子; R 3是H或OH; R 4，R 5，R 6和R 7代表H，NR 10， / SUP> R 11或NH-CO-R 12基团，彼此独立地; 在（i）R 1或R 2中的至少一个为SO 3 R 9的条件下， 和（ii）R 4，R 5，R 6或R 7以及R 7中的至少一个是NR 或其药学上可接受的盐;或其药学上可接受的盐;或其药学上可接受的盐; 和药学上可接受的赋形剂。