公开(公告)号：US07101908B2

公开(公告)日：2006-09-05

申请号：US10690914

申请日：2003-10-22

申请人： Benedikt Sas ,  Johan Van Hemel ,  Jan Vandenkerckhove ,  Eric Peys ,  Johan van der Eycken ,  Bart Ruttens ,  Petra Blom

发明人： Benedikt Sas ,  Johan Van Hemel ,  Jan Vandenkerckhove ,  Eric Peys ,  Johan van der Eycken ,  Bart Ruttens ,  Petra Blom

IPC分类号： A61K31/357 ,  C07D493/04

CPC分类号： C07D493/04 ,  C07D309/10 ,  C07H7/02 ,  C07H7/04 ,  C07H9/04 ,  C07H15/04 ,  C07H15/10 ,  C07H15/203

摘要： Bicyclic carbohydrates for the treatment of infections caused by herpseviridae, and in particular cytomegalovirus. The invention consists of the novel bicyclic carbohydrates the generic structure of which is: wherein R1 is either -Bn or -Ph; R2 and R3 are either -alkyl, -aryl, -allyl, or —H; R4 and R5 form a ring and are either —CH(Ph)- or —CH(aryl)- and X is either O, N or S.

摘要翻译： 双环碳水化合物用于治疗由疱疹病毒科引起的感染，特别是巨细胞病毒。 本发明由新型双环碳水化合物组成，其通用结构为：其中R 1是-Bn或-Ph; R 2和R 3均为 - 烷基， - 芳基， - 烯丙基或-H; R 4和R 5形成环，并且是-CH（Ph） - 或-CH（芳基） - ，X是O，N或S.

公开(公告)号：US07098243B2

公开(公告)日：2006-08-29

申请号：US10663962

申请日：2003-09-16

申请人： Benedikt Sas ,  Johan Van hemel ,  Jan Vandenkerckhove ,  Eric Peys ,  Johan Van Der Eycken ,  Steven Van Hoof

发明人： Benedikt Sas ,  Johan Van hemel ,  Jan Vandenkerckhove ,  Eric Peys ,  Johan Van Der Eycken ,  Steven Van Hoof

IPC分类号： A61K31/70 ,  C07D493/02

CPC分类号： C07D493/02 ,  C07H15/04

摘要： Novel bicyclic carbohydrate compounds are effective for the prophylaxis and treatment of diseases caused by infections of the alphaherpesvirinae HSV-1 and HSV-2. The invention includes the compound wherein X1, X2, and X3 are selected from the group consisting of O, N, and S; wherein Y1 and Y2 are selected from the group consisting of O, N, and S; and wherein Z is selected from the group consisting of F, Cl, and Br, as well as analogs, prodrugs and pharmaceutically acceptable salts thereof, together with pharmaceutical compositions for the prophylaxis and treatment of diseases caused by infections of alphaherpesvirinae.

摘要翻译： 新型双环碳水化合物化合物对于预防和治疗由αherpesvirinaeHSV-1和HSV-2的感染引起的疾病是有效的。 本发明包括其中X 1，X 2和X 3选自O，N和S的化合物; 其中Y 1和Y 2选自O，N和S; 并且其中Z选自F，Cl和Br，以及其类似物，前药和药学上可接受的盐以及用于预防和治疗由αherpesvirinae感染引起的疾病的药物组合物。

公开(公告)号：US20110206636A1

公开(公告)日：2011-08-25

申请号：US12909268

申请日：2010-10-21

申请人： Benedikt Sas ,  Johan Van Hemel ,  Jan Vandenkerckhove ,  Eric Peys ,  Johan Neyts

发明人： Benedikt Sas ,  Johan Van Hemel ,  Jan Vandenkerckhove ,  Eric Peys ,  Johan Neyts

IPC分类号： A61K31/366 ,  A61P31/14 ,  A61K31/39 ,  A61K31/4743 ,  A61K31/55 ,  A61K38/21 ,  A61K31/357

CPC分类号： A61K31/335 ,  A61K31/553 ,  A61K31/554 ,  A61K36/282 ,  A61K38/21 ,  A61K45/06 ,  A61K2300/00

摘要： The use of sesquiterpenes and, in particular sesquiterpene lactone endoperoxides, such as artemisinin and analogs thereof, for the treatment of hepatitis C virus infections. Artemisinin, analogs of artemsisnin and some crude Artemisia extracts were tested in vitro against DNA-viruses, retro-viruses and Flavivirida, (an important family of human and animal RNA pathogens). These compounds were also screened for anti-tumor activity. Strong activity of artemisinin was noticed against the bovine viral diarrhea virus (BVDV). As pestiviruses, such as BVDV, share many similarities with hepatitis C virus (HCV), we can conclude that endoperoxides in general and artemisinin more specifically have efficacy as treatments for hepatitis C viral infections.

摘要翻译： 使用倍半萜烯，特别是倍半萜内酯内过氧化物，如青蒿素及其类似物，用于治疗丙型肝炎病毒感染。 在体外对DNA病毒，逆转录病毒和黄病毒（人类和动物RNA病原体的重要家族）进行体外测定青蒿素，青蒿素类似物和一些粗蒿提取物。 也筛选了这些化合物的抗肿瘤活性。 注意到青蒿素对牛病毒性腹泻病毒（BVDV）的活性较强。 作为瘟病毒，如BVDV，与丙型肝炎病毒（HCV）有许多相似之处，我们可以得出结论，一般的过氧化物和青蒿素更具体地具有作为丙型肝炎病毒感染治疗的功效。

公开(公告)号：US07534871B2

公开(公告)日：2009-05-19

申请号：US10861768

申请日：2004-06-04

申请人： Benedikt Sas ,  Johan van der Eycken ,  Johan Van hemel ,  Petra Blom ,  Jan Vandenkerckhove ,  Bart Ruttens

发明人： Benedikt Sas ,  Johan van der Eycken ,  Johan Van hemel ,  Petra Blom ,  Jan Vandenkerckhove ,  Bart Ruttens

IPC分类号： C07H1/00 ,  C07H17/02

CPC分类号： C07H15/10 ,  C07D309/10 ,  C07D493/04 ,  C07H7/02 ,  C07H7/04 ,  C07H9/04 ,  C07H15/203

摘要： Novel carbohydrate-based compounds with an attached ring system that have antimicrobial or cytostatic activity. The compounds are administered to humans and animals for the treatment or amelioration of bacterial, fungal, viral or protozoal infections or tumors. The compounds are of the general formula:

摘要翻译： 具有附着环系的新型基于碳水化合物的化合物具有抗微生物或抑制细胞活性。 将化合物施用于人和动物以治疗或改善细菌，真菌，病毒或原生动物感染或肿瘤。 该化合物具有以下通式：

公开(公告)号：US07125854B2

公开(公告)日：2006-10-24

申请号：US10752792

申请日：2004-01-07

申请人： Benedikt Sas ,  Johan Van hemel ,  Jan Vandenkerckhove ,  Eric Peys ,  Johan Van der Eycken ,  Bart Ruttens

发明人： Benedikt Sas ,  Johan Van hemel ,  Jan Vandenkerckhove ,  Eric Peys ,  Johan Van der Eycken ,  Bart Ruttens

IPC分类号： A01N43/04 ,  A01N43/16 ,  A61K31/70 ,  A61K31/35

CPC分类号： C07D493/04

摘要： The use of bicyclic carbohydrates for the treatment of parasite infections is described. Different bicyclic carbohydrates have been tested in vitro against a number of protozoa. These compounds also have been screened against viruses, tumors, bacteria and fungi. Compound A1, a thiophenyl-containing bicyclic carbohydrate possessed significant activity against Trypanosoma brucei rhodiense, a parasite that causes the lethal sleeping sickness. Compound A2 and Compound A3, bicyclic carbohydrates with halogen containing aryl groups, possessed significant activity against Leishmania donovani, a parasite that causes leishmaniasis. Bicyclic carbohydrates in general, and Compound A1, Compound A2 and Compound A3 more specifically, could be possible treatments for the sleeping sickness and leishmaniasis in the future.

摘要翻译： 描述了使用双环碳水化合物治疗寄生虫感染。 已经在体外对许多原生动物测试了不同的双环碳水化合物。 这些化合物也已经针对病毒，肿瘤，细菌和真菌进行了筛选。 化合物A1，含噻吩基的双环碳水化合物对引起致死性昏睡病的寄生虫Brucei rhodiense具有显着的活性。 化合物A2和化合物A3，具有含卤素芳基的双环碳水化合物，对引起利什曼病的寄生虫的利什曼原虫（Leishmania donovani）具有显着的活性。 一般来说，双环碳水化合物，化合物A1，化合物A2和化合物A3更具体地可能是今后睡眠病和利什曼病的治疗方法。

公开(公告)号：US20050059647A1

公开(公告)日：2005-03-17

申请号：US10664008

申请日：2003-09-16

申请人： Benedikt Sas ,  Johan hemel ,  Jan Vandenkerckhove ,  Eric Peys

发明人： Benedikt Sas ,  Johan hemel ,  Jan Vandenkerckhove ,  Eric Peys

IPC分类号： A61K31/335 ,  A61K31/55 ,  A61K31/553 ,  A61K31/554 ,  A61K36/282 ,  A61K38/21 ,  A61K45/06

CPC分类号： A61K31/55 ,  A61K31/335 ,  A61K31/553 ,  A61K31/554 ,  A61K36/282 ,  A61K38/21 ,  A61K45/06 ,  A61K2300/00

摘要： The use of sesquiterpenes and, in particular sesquiterpene lactone endoperoxides, such as artemisinin and analogs thereof, for the treatment of hepatitis C virus infections. Artemisinin, analogs of artemsisnin and some crude Artemisia extracts were tested in vitro against DNA-viruses, retro-viruses and Flavivirida, (an important family of human and animal RNA pathogens). These compounds were also screened for anti-tumor activity. Strong activity of artemisinin was noticed against the bovine viral diarrhea virus (BVDV). As pestiviruses, such as BVDV, share many similarities with hepatitis C virus (HCV), we can conclude that endoperoxides in general and artemisinin more specificly have efficacy as treatments for hepatitis C viral infections.

摘要翻译： 使用倍半萜烯，特别是倍半萜内酯内过氧化物，如青蒿素及其类似物，用于治疗丙型肝炎病毒感染。 在体外对DNA病毒，逆转录病毒和黄病毒（人类和动物RNA病原体的重要家族）进行体外测定青蒿素，青蒿素类似物和一些粗蒿提取物。 也筛选了这些化合物的抗肿瘤活性。 注意到青蒿素对牛病毒性腹泻病毒（BVDV）的活性较强。 由于瘟病毒，如BVDV，与丙型肝炎病毒（HCV）有很多相似之处，我们可以得出结论，一般的过氧化物和青蒿素更具体地具有作为丙型肝炎病毒感染治疗的功效。

公开(公告)号：US20080057047A1

公开(公告)日：2008-03-06

申请号：US11605736

申请日：2006-11-28

申请人： Benedikt Sas ,  Johan Van Hemel ,  Jan Vandenkerckhove ,  Eric Peys ,  Hai Tan ,  Chea-Yun Se ,  Chanivilparampu Ramchand ,  Jerry Varghese

发明人： Benedikt Sas ,  Johan Van Hemel ,  Jan Vandenkerckhove ,  Eric Peys ,  Hai Tan ,  Chea-Yun Se ,  Chanivilparampu Ramchand ,  Jerry Varghese

IPC分类号： A61K35/00 ,  A61K31/35 ,  A61P1/00 ,  C12N1/20

CPC分类号： A61K35/742 ,  A23L33/135 ,  A61K38/164 ,  C12R1/07 ,  C12R1/125

摘要： Bacteria of the sp. Bacillus that produce a lipopeptide are found to be effective in the treatment and prophylaxis of gastro-intestinal disease when administered as a probiotic. In particular, a strain of Bacillus bacteria identified as PB6 is useful for the treatment of Antibiotic Associated Diarrhea (AAD) or the more serious condition Clostridium difficile associated diarrhea (CDAD) when administered as a probiotic. Additionally, these bacteria have been found efficient for the treatment of immunorelated diseases such as Inflammatory Bowel Disease (IBD).

摘要翻译： 细菌 发现产生脂肽的芽孢杆菌在作为益生菌施用时可有效地治疗和预防胃肠道疾病。 特别地，当作为益生菌施用时，鉴定为PB6的芽孢杆菌菌株可用于治疗抗生素相关性腹泻（AAD）或更严重的艰难梭菌相关性腹泻（CDAD）。 另外，已经发现这些细菌对于治疗免疫反应性疾病如炎症性肠病（IBD）是有效的。

公开(公告)号：US07138531B2

公开(公告)日：2006-11-21

申请号：US09977478

申请日：2001-10-15

申请人： Benedikt Sas ,  Johan van der Eycken ,  Johan Van hemel ,  Petra Blom ,  Jan Vandenkerckhove ,  Bart Ruttens

发明人： Benedikt Sas ,  Johan van der Eycken ,  Johan Van hemel ,  Petra Blom ,  Jan Vandenkerckhove ,  Bart Ruttens

IPC分类号： C07D493/04

CPC分类号： C07H15/10 ,  C07D309/10 ,  C07D493/04 ,  C07H7/02 ,  C07H7/04 ,  C07H9/04 ,  C07H15/203

摘要： Novel carbohydrate-based compounds with an attached ring system that have antimicrobial or cytostatic activity. The compounds are administered to humans and animals for the treatment or amelioration of bacterial, fungal, viral or protozoal infections or tumors. The compounds are of the general formula:

公开(公告)号：US20050267048A9

公开(公告)日：2005-12-01

申请号：US10690914

申请日：2003-10-22

申请人： Benedikt Sas ,  Johan hemel ,  Jan Vandenkerckhove ,  Eric Peys ,  Johan Eycken ,  Bart Ruttens ,  Petra Blom

发明人： Benedikt Sas ,  Johan hemel ,  Jan Vandenkerckhove ,  Eric Peys ,  Johan Eycken ,  Bart Ruttens ,  Petra Blom

IPC分类号： C07H15/203 ,  A61K31/351 ,  A61K31/357 ,  A61K31/395 ,  A61K31/7034 ,  A61K31/7048 ,  A61K31/7052 ,  A61P31/04 ,  A61P31/10 ,  A61P31/12 ,  A61P33/02 ,  A61P35/00 ,  A61P43/00 ,  C07D309/10 ,  C07D493/04 ,  C07D493/14 ,  C07D498/04 ,  C07H9/00 ,  C07H9/04 ,  C07H13/12 ,  C07H15/04 ,  A61K31/70 ,  A61K31/382 ,  A61K31/445 ,  C07D211/36

CPC分类号： C07D493/04 ,  C07D309/10 ,  C07H7/02 ,  C07H7/04 ,  C07H9/04 ,  C07H15/04 ,  C07H15/10 ,  C07H15/203

摘要： Bicyclic carbohydrates for the treatment of infections caused by herpseviridae, and in particular cytomegalovirus. The invention consists of the novel bicyclic carbohydrates the generic structure of which is: wherein R1 is either -Bn or -Ph; R2 and R3 are either -alkyl, -aryl, -allyl, or —H; R4 and R5 form a ring and are either —CH(Ph)- or —CH(aryl)- and X is either O, N or S.

公开(公告)号：US20050059612A1

公开(公告)日：2005-03-17

申请号：US10663962

申请日：2003-09-16

申请人： Benedikt Sas ,  Johan hemel ,  Jan Vandenkerckhove ,  Eric Peys ,  Johan Eycken ,  Steven Hoof

发明人： Benedikt Sas ,  Johan hemel ,  Jan Vandenkerckhove ,  Eric Peys ,  Johan Eycken ,  Steven Hoof

IPC分类号： C07D493/02 ,  C07H15/04 ,  A61K31/70

CPC分类号： C07D493/02 ,  C07H15/04

摘要： Novel bicyclic carbohydrate compounds are effective for the prophylaxis and treatment of diseases caused by infections of the alphaherpesvirinae HSV-1 and HSV-2. The invention includes the compound wherein X1, X2, and X3 are selected from the group consisting of O, N, and S; wherein Y1 and Y2 are selected from the group consisting of O, N, and S; and wherein Z is selected from the group consisting of F, Cl, and Br, as well as analogs, prodrugs and pharmaceutically acceptable salts thereof, together with pharmaceutical compositions for the prophylaxis and treatment of diseases caused by infections of alphaherpesvirinae.

摘要翻译： 新型双环碳水化合物化合物对于预防和治疗由αherpesvirinaeHSV-1和HSV-2的感染引起的疾病是有效的。 本发明包括其中X 1，X 2和X 3选自O，N和S的化合物; 其中Y1和Y2选自O，N和S; 并且其中Z选自F，Cl和Br，以及其类似物，前药和药学上可接受的盐以及用于预防和治疗由αherpesvirinae感染引起的疾病的药物组合物。