公开(公告)号：US07786142B2

公开(公告)日：2010-08-31

申请号：US11546299

申请日：2006-10-12

申请人： Siripragada Mahender Rao ,  Akella Satya Surya Visweswara Srinvas ,  Shikha Rani ,  Gaddam Om Reddy ,  Sriram Rajagopal ,  Uma Ramachandran ,  Duddu Savaraiah Sharada ,  Rajagopalan Nirmala ,  Velaiah Sivasudar ,  Lakshmanan Manikandan ,  Ramachandran Balaji

发明人： Siripragada Mahender Rao ,  Akella Satya Surya Visweswara Srinvas ,  Shikha Rani ,  Gaddam Om Reddy ,  Sriram Rajagopal ,  Uma Ramachandran ,  Duddu Savaraiah Sharada ,  Rajagopalan Nirmala ,  Velaiah Sivasudar ,  Lakshmanan Manikandan ,  Ramachandran Balaji

IPC分类号： A61K31/4468 ,  A61K31/403 ,  C07D405/14 ,  C07D209/88

CPC分类号： C07D209/88 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D417/12

摘要： The present invention relates to novel heterocyclic compounds of the general formula (I), as IL-6 inhibitors, their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their hydrates, their solvates, their pharmaceutically acceptable salts and compositions, their metabolites and prodrugs thereof. The present invention more particularly provides novel heterocyclic compounds of the general formula (I). Also included is a method for treatment of cancer, cancer cachexia and inflammatory diseases including immunological diseases, particularly those mediated by cytokines such as IL-6, through pSTAT3 inhibition, in a mammal comprising administering an effective amount of a compound of formula (I) as described above

摘要翻译： 本发明涉及通式（I）的新型杂环化合物，作为IL-6抑制剂，其衍生物，其类似物，其互变异构形式，其立体异构体，其多晶型物，其水合物，其溶剂合物，其药学上可接受的盐和组合物 ，它们的代谢物和前药。 本发明更具体地提供了通式（I）的新型杂环化合物。 还包括在哺乳动物中治疗癌症，癌症恶病质和炎性疾病的方法，包括免疫疾病，特别是通过pSTAT3抑制的细胞因子如IL-6介导的疾病，包括给予有效量的式（I）化合物， 如上所述

公开(公告)号：US07687488B2

公开(公告)日：2010-03-30

申请号：US11822956

申请日：2007-07-11

申请人： Senthilkumar Udayampalayam Palanisamy ,  Andrew Gnanaprakasam ,  Panchapakesan Ganapathy ,  Mukut Gohain ,  Venkatasubramanian Hariharan ,  Sriram Rajagopal ,  Maneesh Paul-Satyaseela ,  Shakti Singh Solanki ,  Sathishkumar Devarajan

发明人： Senthilkumar Udayampalayam Palanisamy ,  Andrew Gnanaprakasam ,  Panchapakesan Ganapathy ,  Mukut Gohain ,  Venkatasubramanian Hariharan ,  Sriram Rajagopal ,  Maneesh Paul-Satyaseela ,  Shakti Singh Solanki ,  Sathishkumar Devarajan

IPC分类号： A61K31/43 ,  C07D499/00

CPC分类号： C07D499/86 ,  Y02P20/55

摘要： Novel 2-substituted methyl penam derivatives include the formula (I), their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their solvates, their pharmaceutically acceptable salts, and pharmaceutical compositions containing them; wherein A=C or N; Het is a three- to seven-membered heterocyclic ring; R1 represents carboxylate anion, or —COOR4 where R4 represents hydrogen, carboxylic acid protecting group or a pharmaceutically acceptable salt; R2 and R3 may be same or different and independently represent hydrogen, halogen, amino, alkyl, protected amino, optionally substituted alkyl, alkenyl, alkynyl and the like; R represents substituted or unsubstituted alkyl, alkenyl, aryl, aralkyl, cycloalkyl, heterocyclyl or heterocyclylalkyl.

摘要翻译： 新的2-取代的甲基penam衍生物包括式（I），它们的类似物，它们的互变异构形式，它们的立体异构体，它们的多晶型物，它们的溶剂合物，其药学上可接受的盐和含有它们的药物组合物; 其中A = C或N; Het是一个三至七元的杂环; R1表示羧酸根阴离子，或-COOR4，其中R4表示氢，羧酸保护基或药学上可接受的盐; R2和R3可以相同或不同，并且独立地表示氢，卤素，氨基，烷基，保护的氨基，任选取代的烷基，烯基，炔基等; R代表取代或未取代的烷基，烯基，芳基，芳烷基，环烷基，杂环基或杂环基烷基。

公开(公告)号：US20080221103A1

公开(公告)日：2008-09-11

申请号：US12073635

申请日：2008-03-07

申请人： Ganapavarapu V.R. Sharma ,  Gaddam O. Reddy ,  Sriram Rajagopal ,  Uma Ramachandran ,  Sukunath Narayanan ,  Nagalakshmi Pichika ,  Venkatesh Nemmara Viswanathan ,  Lavanya Andiappan ,  Saravanan Thirunavukkarasu

发明人： Ganapavarapu V.R. Sharma ,  Gaddam O. Reddy ,  Sriram Rajagopal ,  Uma Ramachandran ,  Sukunath Narayanan ,  Nagalakshmi Pichika ,  Venkatesh Nemmara Viswanathan ,  Lavanya Andiappan ,  Saravanan Thirunavukkarasu

IPC分类号： A61K31/5377 ,  C07D239/24 ,  C07D413/14 ,  A61K31/435 ,  A61P37/06

CPC分类号： C07D239/24 ,  C07D413/14

摘要： Provided herein are heterocyclic compounds of the general formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts and compositions, metabolites and prodrugs thereof, wherein R1, R2, R3, R4 and R5 are as described herein. Further described herein in particular are heterocyclic compounds of the formula (I) for treating various diseases. and disorders by administering in a patient one or more TNF-α, Thromboxane synthase, 5-LOX, and PDE4 inhibitors. In particular described herein are methods for treating immunological diseases, inflammation, pain disorder, rheumatoid arthritis; osteoporosis; multiple myeloma; uveititis; acute and chronic myelogenous leukemia; ischemic heart disease; atherosclerosis; cancer; ischemic-induced cell damage; pancreatic beta cell destruction; osteoarthritis; rheumatoid spondylitis; gouty arthritis; inflammatory bowel disease; adult respiratory distress syndrome (ARDS); psoriasis; Crohn's disease; allergic rhinitis; ulcerative colitis; anaphylaxis; contact dermatitis; muscle degeneration; cachexia; asthma; bone resorption diseases; ischemia reperfusion injury; brain trauma; multiple sclerosis; sepsis; septic shock; toxic shock syndrome; fever, and myalgias due to infection and diseases mediated by HIV-1; HIV-2; HIV-3; cytomegalovirus (CMV); influenza; adenovirus; the herpes viruses (including HSV-1, HSV-2) and herpes zoster viruses in a mammal comprising administering an effective amount of a compound of formula (I).

摘要翻译： 本文提供了通式（I）的杂环化合物，其衍生物，类似物，互变异构形式，立体异构体，多晶型物，水合物，溶剂合物，药学上可接受的盐和组合物，其代谢物和前药，其中R 1， R 2，R 3，R 4和R 5如本文所述。 本文进一步描述的是用于治疗各种疾病的式（I）的杂环化合物。 以及通过在患者中施用一种或多种TNF-α，血栓烷合成酶，5-LOX和PDE4抑制剂的障碍。 本文特别描述的是用于治疗免疫疾病，炎症，疼痛障碍，类风湿性关节炎的方法; 骨质疏松症 多发性骨髓瘤 葡萄膜炎 急性和慢性粒细胞白血病; 缺血性心脏病; 动脉粥样硬化 癌症; 缺血诱导的细胞损伤; 胰腺β细胞破坏; 骨关节炎 类风湿性脊柱炎; 痛风性关节炎 炎症性肠病; 成人呼吸窘迫综合征（ARDS）; 银屑病; 克罗恩病; 过敏性鼻炎; 溃疡性结肠炎 过敏反应 接触性皮炎; 肌肉退化; 恶病质 哮喘; 骨吸收疾病; 缺血再灌注损伤; 脑外伤; 多发性硬化症 脓毒症 败血性休克 中毒性休克综合征; 发热和由于HIV-1介导的感染和疾病引起的肌痛; HIV-2; HIV-3; 巨细胞病毒（CMV）; 流感; 腺病毒 哺乳动物中的疱疹病毒（包括HSV-1，HSV-2）和带状疱疹病毒，包括施用有效量的式（I）化合物。

公开(公告)号：US20080015156A1

公开(公告)日：2008-01-17

申请号：US11822956

申请日：2007-07-11

申请人： Senthilkumar Udayampalayam Palanisamy ,  Andrew Gnanaprakasam ,  Panchapakesan Ganapathy ,  Mukut Gohain ,  Venkatasubramanian Hariharan ,  Sriram Rajagopal ,  Maneesh Paul-Satyaseela ,  Shakti Solanki ,  Sathishkumar Devarajan

发明人： Senthilkumar Udayampalayam Palanisamy ,  Andrew Gnanaprakasam ,  Panchapakesan Ganapathy ,  Mukut Gohain ,  Venkatasubramanian Hariharan ,  Sriram Rajagopal ,  Maneesh Paul-Satyaseela ,  Shakti Solanki ,  Sathishkumar Devarajan

IPC分类号： A61K31/431 ,  A61K31/7036 ,  A61P31/00 ,  C07D499/00

CPC分类号： C07D499/86 ,  Y02P20/55

摘要： Novel 2-substituted methyl penam derivatives include the formula (I), their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their solvates, their pharmaceutically acceptable salts, and pharmaceutical compositions containing them; wherein A=C or N; Het is a three- to seven-membered heterocyclic ring; R1 represents carboxylate anion, or —COOR4 where R4 represents hydrogen, carboxylic acid protecting group or a pharmaceutically acceptable salt; R2 and R3 may be same or different and independently represent hydrogen, halogen, amino, alkyl, protected amino, optionally substituted alkyl, alkenyl, alkynyl and the like; R represents substituted or unsubstituted alkyl, alkenyl, aryl, aralkyl, cycloalkyl, heterocyclyl or heterocyclylalkyl.

摘要翻译： 新的2-取代的甲基penam衍生物包括式（I），它们的类似物，它们的互变异构形式，它们的立体异构体，它们的多晶型物，它们的溶剂合物，其药学上可接受的盐和含有它们的药物组合物; 其中A = C或N; Het是一个三至七元的杂环; R 1表示羧酸根阴离子或-COOR 4，其中R 4表示氢，羧酸保护基或其药学上可接受的盐; R 2和R 3可以相同或不同，并且独立地表示氢，卤素，氨基，烷基，保护的氨基，任选取代的烷基，烯基，炔基等; R代表取代或未取代的烷基，烯基，芳基，芳烷基，环烷基，杂环基或杂环基烷基。

公开(公告)号：US06576662B2

公开(公告)日：2003-06-10

申请号：US09849584

申请日：2001-05-04

申请人： Srinivas Nanduri ,  Sriram Rajagopal ,  Venkateswarlu Akella

发明人： Srinivas Nanduri ,  Sriram Rajagopal ,  Venkateswarlu Akella

IPC分类号： A61K3134

CPC分类号： C07D405/06 ,  C07D307/58 ,  C07D405/08 ,  C07D405/12 ,  C07D417/12

摘要： The present invention relates to novel anticancer agents, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, and their pharmaceutically acceptable solvates. The present invention more particularly relates to novel derivatives of andrographolide, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, and their pharmaceutically acceptable solvates. The novel derivatives of andrographolide have the general formula (I).

公开(公告)号：US10285655B2

公开(公告)日：2019-05-14

申请号：US14002787

申请日：2012-03-09

申请人： Shufang Dong ,  Terrance Joseph Nemenz ,  Patrick Cumpson ,  Jeremy David Pettinato ,  Sriram Rajagopal

发明人： Shufang Dong ,  Terrance Joseph Nemenz ,  Patrick Cumpson ,  Jeremy David Pettinato ,  Sriram Rajagopal

IPC分类号： A61B6/00 ,  A61B6/03 ,  A61B6/04 ,  A61B6/10 ,  A61B5/055

摘要： A method includes receiving a subject support motion disable signal indicative of at least one of power removal of an imaging system, a collision of a horizontally moving tabletop of the imaging system, a decoupling of a horizontal motion drive system configured to horizontally drive the tabletop, or a collision of a vertically moving subject support of the imaging system, wherein a vertical motion drive system drives the subject support vertical motion, and disabling, in response to receiving the subject support motion disable signal, at least one of tabletop horizontal motion or subject support vertical motion.

公开(公告)号：US08420653B2

公开(公告)日：2013-04-16

申请号：US12863796

申请日：2009-01-30

申请人： Visweswara Akella Satya Surya Srinivas ,  Ravikumar Tadiparthi ,  Ganapavarapu Veera Raghava Sharma ,  Thirunavukkarasu Sappanimuthu ,  Durairaj Peter Bhakiaraj ,  Virendra Kachhadia ,  Kilambi Narasimhan ,  Sathya Narayana Thara ,  Sriram Rajagopal ,  Sukunath Narayanan ,  Venkatesan Parameswaran ,  Venkatesan Janarthanam ,  Maruthikumar Narayanam ,  Sathyanarayana Gadde ,  Uma Ramachandran ,  Gopalan Balasubramanian ,  Narayanan Surendran ,  Shridhar Narayanan ,  Lolaknath Santosh Vishwakarma ,  Sanjeev Saxena ,  Nishikanth Reddy Gaddam

发明人： Visweswara Akella Satya Surya Srinivas ,  Ravikumar Tadiparthi ,  Ganapavarapu Veera Raghava Sharma ,  Thirunavukkarasu Sappanimuthu ,  Durairaj Peter Bhakiaraj ,  Virendra Kachhadia ,  Kilambi Narasimhan ,  Sathya Narayana Thara ,  Sriram Rajagopal ,  Om Reddy Gaddam ,  Sukunath Narayanan ,  Venkatesan Parameswaran ,  Venkatesan Janarthanam ,  Maruthikumar Narayanam ,  Sathyanarayana Gadde ,  Uma Ramachandran ,  Gopalan Balasubramanian ,  Narayanan Surendran ,  Shridhar Narayanan ,  Lolaknath Santosh Vishwakarma ,  Sanjeev Saxena

IPC分类号： A01N43/54 ,  C07D239/42 ,  C07D401/04

CPC分类号： C07D239/42 ,  A61K31/5377 ,  C07D265/28 ,  C07D401/04

摘要： Described are novel heterocyclic compounds of the general formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts, pharmaceutical compositions, metabolites and prodrugs thereof. These compounds are useful in the treatment of immunological diseases, inflammation, pain disorder, rheumatoid arthritis; osteoporosis; multiple myeloma; uveititis; acute and chronic myelogenous leukemia; atherosclerosis; cancer; cachexia; ischemic-induced cell damage; pancreatic beta cell destruction; osteoarthritis; rheumatoid spondylitis; gouty arthritis; inflammatory bowel disease; ARDS; psoriasis; Crohn's disease; allergic rhinitis; ulcerative colitis; anaphylaxis; contact dermatitis; muscle degeneration; asthma; COPD; bone resorption diseases; multiple sclerosis; sepsis; septic shock; toxic shock syndrome and fever. More particularly these compounds are useful as PDE4 inhibitors and are useful for treating PDE4 mediated diseases.

摘要翻译： 描述了通式（I）的新型杂环化合物，其衍生物，类似物，互变异构形式，立体异构体，多晶型物，水合物，溶剂合物，药学上可接受的盐，药物组合物，代谢物和前药。 这些化合物可用于治疗免疫疾病，炎症，疼痛障碍，类风湿性关节炎; 骨质疏松症 多发性骨髓瘤 葡萄膜炎 急性和慢性粒细胞白血病; 动脉粥样硬化 癌症; 恶病质 缺血诱导的细胞损伤; 胰腺β细胞破坏; 骨关节炎 类风湿性脊柱炎; 痛风性关节炎 炎症性肠病; ARDS; 银屑病; 克罗恩病; 过敏性鼻炎; 溃疡性结肠炎 过敏反应 接触性皮炎; 肌肉退化; 哮喘; COPD; 骨吸收疾病; 多发性硬化症 败血症 败血性休克 中毒性休克综合征和发烧。 更特别地，这些化合物可用作PDE4抑制剂，并且可用于治疗PDE4介导的疾病。

公开(公告)号：US08263044B2

公开(公告)日：2012-09-11

申请号：US12084430

申请日：2006-11-06

申请人： Akella Satya Surya Visweswara Srinivas ,  Urkalan Kaveri Balan ,  Narayana Swamy Punthalir ,  Rama Swamy Velmurugan ,  Sriram Rajagopal ,  Gaddam Om Reddy ,  Virendra Kachhadia

发明人： Akella Satya Surya Visweswara Srinivas ,  Urkalan Kaveri Balan ,  Narayana Swamy Punthalir ,  Rama Swamy Velmurugan ,  Sriram Rajagopal ,  Gaddam Om Reddy ,  Virendra Kachhadia

IPC分类号： A61K9/12 ,  A61K31/427 ,  A61K31/4409 ,  C07D417/04 ,  C07D213/56 ,  A61P35/00

CPC分类号： C07C259/06 ,  C07C237/22 ,  C07C323/62 ,  C07D213/56 ,  C07D277/30 ,  C07D277/46 ,  C07D277/58 ,  C07D277/82 ,  C07D307/56 ,  C07D333/24 ,  C07D333/28 ,  C07D417/06

摘要： The present invention relates to novel stilbene like compounds of the general formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts and compositions, metabolites and prodrugs thereof. The present invention more particularly provides novel stilbene like compounds of the general formula (I). Also included is a method for treatment of cancer, psoriasis, proliferative conditions and conditions mediated by HDAC, in a mammal comprising administering an effective amount of a novel compound of formula (I) as described above.

摘要翻译： 本发明涉及通式（I）的新颖的二苯乙烯类化合物，其衍生物，类似物，互变异构形式，立体异构体，多晶型物，水合物，溶剂合物，药学上可接受的盐和组合物，其代谢物和前药。 本发明更具体地提供了通式（I）的新颖的二苯乙烯类化合物。 还包括在哺乳动物中治疗癌症，牛皮癣，增殖性病症和由HDAC介导的病症的方法，包括给予有效量的如上所述的新的式（I）化合物。

公开(公告)号：US08080559B2

公开(公告)日：2011-12-20

申请号：US12577399

申请日：2009-10-12

申请人： Venkateswarlu Akella ,  Shanavas Alikunju ,  Ajaya Kumar Reka ,  Ramesh Mullangi ,  Raju Sirisilla ,  Subrahmanyam Duvvuri ,  Sriram Rajagopal

发明人： Venkateswarlu Akella ,  Shanavas Alikunju ,  Ajaya Kumar Reka ,  Ramesh Mullangi ,  Raju Sirisilla ,  Subrahmanyam Duvvuri ,  Sriram Rajagopal

IPC分类号： A61K31/4745 ,  C07D491/22

CPC分类号： C07D491/22 ,  C07D519/00

摘要： A 5(S)-(2′-hydroxyethoxy)-20(S)-camptothecin diasterisomer is described which is a better inhibitor of topoisomerase I than either the diastereoisomeric mixture 5(RS)-(2′-hydroxyethoxy)-20(S)-camptothecin, or the 5(R)-(2′-hydroxyethoxy)-20(S)-camptothecin diastereoisomer. Pharmaceutical compositions of the 5(S)-(2′-hydroxyethoxy)-20(S)-camptothecin diastereoisomer are also described as are methods of using the compound for the inhibition of topoisomerase I and for the treatment of cancer.

摘要翻译： 描述了5（S） - （2'-羟基乙氧基）-20（S） - 喜树碱非对映异构体，其是非对映异构体混合物5（RS） - （2'-羟基乙氧基）-20（S ） - 喜树碱或5（R） - （2'-羟基乙氧基）-20（S） - 喜树碱非对映异构体。 还描述了5（S） - （2'-羟基乙氧基）-20（S） - 喜树碱非对映异构体的药物组合物是使用该化合物抑制拓扑异构酶I和治疗癌症的方法。

公开(公告)号：US20100222379A1

公开(公告)日：2010-09-02

申请号：US12734026

申请日：2008-10-08

申请人： Sridharan Rajagopal ,  Virendra Kachhadia ,  Thanasekaran Ponpandian ,  Abdul Raheem Keeri ,  Umamaheswari Mani ,  Suresh Rathinasamy ,  Praveen Rajendran ,  Kamaraj Mani ,  Balaji Ramachandran ,  Punthalir Narayanaswamy ,  Sriram Rajagopal

发明人： Sridharan Rajagopal ,  Virendra Kachhadia ,  Thanasekaran Ponpandian ,  Abdul Raheem Keeri ,  Umamaheswari Mani ,  Suresh Rathinasamy ,  Praveen Rajendran ,  Kamaraj Mani ,  Balaji Ramachandran ,  Punthalir Narayanaswamy ,  Sriram Rajagopal

IPC分类号： A61K31/167 ,  C07C237/40 ,  C07D215/38 ,  A61K31/47 ,  A61P35/00

CPC分类号： C07C237/42 ,  C07C237/22 ,  C07C259/06 ,  C07C259/10 ,  C07C271/22 ,  C07C275/50 ,  C07C2601/02 ,  C07D213/56 ,  C07D215/14 ,  C07D317/60 ,  C07D333/24 ,  C07D333/44

摘要： Provided herein are novel, stilbene like compounds of the general formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, metabolites, prodrugs, solvates, pharmaceutically acceptable salts and compositions thereof. These compounds can inhibit HDACs and are useful as a therapeutic or ameliorating agent for diseases that are involved in cellular growth such as WO 2009/047615 A2 malignant tumors, autoimmune diseases, skin diseases, infections, inflammation, etc.

摘要翻译： 本文提供了新颖的通式（I）的二苯乙烯类化合物，其衍生物，类似物，互变异构形式，立体异构体，多晶型物，水合物，代谢物，前药，溶剂化物，药学上可接受的盐和组合物。 这些化合物可以抑制HDAC，并且可用作涉及细胞生长的疾病的治疗或改善剂，例如WO 2009/047615A2恶性肿瘤，自身免疫性疾病，皮肤病，感染，炎症等。