公开(公告)号：US08686028B2

公开(公告)日：2014-04-01

申请号：US13127913

申请日：2009-05-14

申请人： Atul Goel ,  Amit Kumar ,  Sumit Chaurasia ,  Divya Singh ,  Abnish Kumar Gautam ,  Rashmi Pandey ,  Ritu Trivedi ,  Man Mohan Singh ,  Naibedya Chattopadhyay ,  Lakshmi Manickavasagam ,  Girish Kumar Jain ,  Anil Kumar Dwivedi

发明人： Atul Goel ,  Amit Kumar ,  Sumit Chaurasia ,  Divya Singh ,  Abnish Kumar Gautam ,  Rashmi Pandey ,  Ritu Trivedi ,  Man Mohan Singh ,  Naibedya Chattopadhyay ,  Lakshmi Manickavasagam ,  Girish Kumar Jain ,  Anil Kumar Dwivedi

IPC分类号： A61K31/352 ,  A61K31/4453 ,  C07D311/36 ,  C07D493/04

CPC分类号： C07D493/04 ,  C07D311/36

摘要： The present invention relates to novel substituted benzfurochromenes and related compounds having the general formula (I), salts and chiral, achiral derivatives thereof; wherein R1, R2, R3, R4, R5, R6, R7, R8 are independently selected from the groups consisting of hydrogen, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkoxyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted alkylthio, optionally substituted amino, optionally substituted acylamino, optionally substituted arylamino, optionally substituted acylthio, optionally substituted acyl, optionally substituted aroyl, optionally substituted acyloxy, optionally substituted thioamido, halogens, nitriles, esters, hydroxy, mercapto, carbontrifluoride, nitro but not limited to this; wherein R1R2 or R2R3 or R6R7 may be connected and form either a five membered ring or a six membered ring such as optionally substituted furan, optionally substituted dihydrofuran, optionally substituted pyran; or may be connected through a methylenedeoxy moiety; wherein X is selected from the units consisting of optionally a ketone group, optionally a methylene group, optionally substituted methylene group, optionally substituted alkene; wherein Y and Z is selected from the units consisting of CH, C—OH, C-Me, C—OMe with the proviso that bond between Y and Z is a single bond; Wherein Y and Z may be a carbon atom with the proviso that bond between Y and Z is a double bond. The compounds of the general formula is useful for the prevention and treatment of bone related disorders.

摘要翻译： 本发明涉及具有通式（I）的新型取代的苯并呋喃和其相关化合物，其盐和手性的非手性衍生物; 其中R1，R2，R3，R4，R5，R6，R7，R8独立地选自氢，任选取代的烷基，任选取代的烯基，任选取代的烷氧基，任选取代的芳基，任选取代的杂芳基，任选取代的烷硫基， 任选取代的氨基，任选取代的酰基氨基，任选取代的芳基氨基，任选取代的酰基硫基，任选取代的酰基，任选取代的芳酰基，任选取代的酰氧基，任选取代的硫代酰氨基，卤素，腈，酯，羟基，巯基，三氟化碳，硝基，但不限于此 ; 其中R1R2或R2R3或R6R7可以连接并形成五元环或六元环，例如任选取代的呋喃，任选取代的二氢呋喃，任选取代的吡喃; 或可以通过亚甲二氧基部分连接; 其中X选自由任选的酮基，任选的亚甲基，任选取代的亚甲基，任选取代的烯烃组成的单元; 其中Y和Z选自由CH，C-OH，C-Me，C-OMe组成的单元，条件是Y和Z之间的键是单键; 其中Y和Z可以是碳原子，条件是Y和Z之间的键是双键。 通式的化合物可用于预防和治疗骨相关疾病。

公开(公告)号：US20120003273A1

公开(公告)日：2012-01-05

申请号：US13127913

申请日：2009-05-14

申请人： Atul Goel ,  Amit Kumar ,  Sumit Chaurasia ,  Divya Singh ,  Abnish Kumar Gautam ,  Rashmi Pandey ,  Ritu Trivedi ,  Man Mohan Singh ,  Naibedya Chattopadhyay ,  Lakshmi Manickavasagam ,  Girish Kumar Jain ,  Anil Kumar Dwivedi

发明人： Atul Goel ,  Amit Kumar ,  Sumit Chaurasia ,  Divya Singh ,  Abnish Kumar Gautam ,  Rashmi Pandey ,  Ritu Trivedi ,  Man Mohan Singh ,  Naibedya Chattopadhyay ,  Lakshmi Manickavasagam ,  Girish Kumar Jain ,  Anil Kumar Dwivedi

IPC分类号： A61K31/352 ,  C07D311/36 ,  A61P19/08 ,  A61K31/4453 ,  A61P19/10 ,  C07D493/04 ,  A61K9/00

CPC分类号： C07D493/04 ,  C07D311/36

摘要： The present invention relates to novel substituted benzfurochromenes and related compounds having the general formula (I), salts and chiral, achiral derivatives thereof; wherein R1, R2, R3, R4, R5, R6, R7, R8 are independently selected from the groups consisting of hydrogen, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkoxyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted alkylthio, optionally substituted amino, optionally substituted acylamino, optionally substituted arylamino, optionally substituted acylthio, optionally substituted acyl, optionally substituted aroyl, optionally substituted acyloxy, optionally substituted thioamido, halogens, nitriles, esters, hydroxy, mercapto, carbontrifluoride, nitro but not limited to this; wherein R1R2 or R2R3 or R6R7 may be connected and form either a five membered ring or a six membered ring such as optionally substituted furan, optionally substituted dihydrofuran, optionally substituted pyran; or may be connected through a methylenedeoxy moiety; wherein X is selected from the units consisting of optionally a ketone group, optionally a methylene group, optionally substituted methylene group, optionally substituted alkene; wherein Y and Z is selected from the units consisting of CH, C—OH, C-Me, C—OMe with the proviso that bond between Y and Z is a single bond; Wherein Y and Z may be a carbon atom with the proviso that bond between Y and Z is a double bond. The compounds of the general formula is useful for the prevention and treatment of bone related disorders.

摘要翻译： 本发明涉及具有通式（I）的新型取代的苯并呋喃和其相关化合物，其盐和手性的非手性衍生物; 其中R1，R2，R3，R4，R5，R6，R7，R8独立地选自氢，任选取代的烷基，任选取代的烯基，任选取代的烷氧基，任选取代的芳基，任选取代的杂芳基，任选取代的烷硫基， 任选取代的氨基，任选取代的酰基氨基，任选取代的芳基氨基，任选取代的酰基硫基，任选取代的酰基，任选取代的芳酰基，任选取代的酰氧基，任选取代的硫代酰氨基，卤素，腈，酯，羟基，巯基，三氟化碳，硝基，但不限于此 ; 其中R1R2或R2R3或R6R7可以连接并形成五元环或六元环，例如任选取代的呋喃，任选取代的二氢呋喃，任选取代的吡喃; 或可以通过亚甲二氧基部分连接; 其中X选自由任选的酮基，任选的亚甲基，任选取代的亚甲基，任选取代的烯烃组成的单元; 其中Y和Z选自由CH，C-OH，C-Me，C-OMe组成的单元，条件是Y和Z之间的键是单键; 其中Y和Z可以是碳原子，条件是Y和Z之间的键是双键。 通式的化合物可用于预防和治疗骨相关疾病。

公开(公告)号：US20110112042A1

公开(公告)日：2011-05-12

申请号：US12920927

申请日：2009-03-03

申请人： Rakesh Maurya ,  Preeti Rawat ,  Kunal Sharan ,  Jawed Akhtar Siddiqui ,  Gaurav Swarnkar ,  Geetanjali Mishra ,  Lakshmi Manickavasagam ,  Girish Kumar Jain ,  Kamal Ram Arya ,  Naibedya Chattopadhyay

发明人： Rakesh Maurya ,  Preeti Rawat ,  Kunal Sharan ,  Jawed Akhtar Siddiqui ,  Gaurav Swarnkar ,  Geetanjali Mishra ,  Lakshmi Manickavasagam ,  Girish Kumar Jain ,  Kamal Ram Arya ,  Naibedya Chattopadhyay

IPC分类号： A61K31/7048 ,  C07H7/06 ,  C07H1/08 ,  A61P19/08

CPC分类号： C07H7/06 ,  C07D405/04

摘要： The present invention provides a flavonol compound and a bioactive extract/fraction from Ulmus wallichiana useful for the management or prevention or treatment of bone disorders. Said extract/fraction comprising marker compounds of general formula 2, K058: R1═R2═0H K012: R1═R2═OH, 2,3 double bond K068: R1═R2═H KIOOi R1═OH, R2═H mula 2 Wherein the marker compounds K012, K058, K068, K100 ranges 6.7-12%, 1.7-4.5%, 0.6-1.2%, 1.7-4.5% respectively in alcoholic extract and a process of extraction thereof. According to another aspect of the invention provides a pharmaceutical composition comprising the said compound. The present invention further provides a method of treating bone disorders by administering the pharmaceutical composition by oral, intravenous, subcutaneous, intra-peritoneal or intramuscular route.

摘要翻译： 本发明提供了一种黄酮醇化合物和可用于治疗或预防或治疗骨骼疾病的来自榆树的生物活性提取物/部分。 所述提取物/级分包含通式2的标记化合物，K058：R1 = R2 = 0H，K012：R1 = R2 = OH，2,3双键，K068：R1 = R2 = H，KIOO，R1 = OH，R2 = H， 标记化合物K012，K058，K068，K100分别在酒精提取物中分别为6.7-12％，1.7-4.5％，0.6-1.2％，1.7-4.5％及其提取方法。 根据本发明的另一方面，提供了包含所述化合物的药物组合物。 本发明还提供了通过口服，静脉内，皮下，腹膜内或肌肉内途径施用药物组合物来治疗骨病的方法。

公开(公告)号：US08669232B2

公开(公告)日：2014-03-11

申请号：US12920927

申请日：2009-03-03

申请人： Rakesh Maurya ,  Preeti Rawat ,  Kunal Sharan ,  Jawed Akhtar Siddiqui ,  Gaurav Swarnkar ,  Geetanjali Mishra ,  Lakshmi Manickavasagam ,  Girish Kumar Jain ,  Kamal Ram Arya ,  Naibedya Chattopadhyay

发明人： Rakesh Maurya ,  Preeti Rawat ,  Kunal Sharan ,  Jawed Akhtar Siddiqui ,  Gaurav Swarnkar ,  Geetanjali Mishra ,  Lakshmi Manickavasagam ,  Girish Kumar Jain ,  Kamal Ram Arya ,  Naibedya Chattopadhyay

IPC分类号： A61K31/70 ,  A61K31/7028 ,  A61K31/7042 ,  C07H1/08

CPC分类号： C07H7/06 ,  C07D405/04

摘要： The present invention provides a flavonol compound and a bioactive extract/fraction from Ulmus wallichiana useful for the management or prevention or treatment of bone disorders. Said extract/fraction comprising marker compounds of general formula 2, K058: R1═R2═OH K012: R1═R2═OH, 2,3 double bond K068: R1═R2═H KIOOi R1═OH, R2═H mula 2 Wherein the marker compounds K012, K058, K068, K1OO ranges 6.7-12%, 1.7-4.5%, 0.6-1.2%, 1.7-4.5% respectively in alcoholic extract and a process of extraction thereof. According to another aspect of the invention provides a pharmaceutical composition comprising the said compound. The present invention further provides a method of treating bone disorders by administering the pharmaceutical composition by oral, intravenous, subcutaneous, intra-peritoneal or intramuscular route.

摘要翻译： 本发明提供了一种黄酮醇化合物和可用于治疗或预防或治疗骨骼疾病的来自榆树的生物活性提取物/部分。 所述提取物/级分包含通式2的标记化合物，K058：R1 = R2 = OHK012：R1 = R2 = OH，2,3双键K068：R1 = R2 = H KIOOi R1 = OH，R2 = Hmula 2其中 标记化合物K012，K058，K068，K100分别在酒精提取物中分别为6.7-12％，1.7-4.5％，0.6-1.2％，1.7-4.5％及其提取方法。 根据本发明的另一方面，提供了包含所述化合物的药物组合物。 本发明还提供了通过口服，静脉内，皮下，腹膜内或肌肉内途径施用药物组合物来治疗骨病的方法。