公开(公告)号：US20070072876A1

公开(公告)日：2007-03-29

申请号：US11516549

申请日：2006-09-07

Applicant: Ravikumar Tadiparthi ,  Venkatesan Parameswaran ,  Rajib Barik ,  Gaddam Reddy ,  Pawan Aggarwal ,  Sappanimuthu Thirunavukkarasu ,  Sriram Rajagopal

Inventor： Ravikumar Tadiparthi ,  Venkatesan Parameswaran ,  Rajib Barik ,  Gaddam Reddy ,  Pawan Aggarwal ,  Sappanimuthu Thirunavukkarasu ,  Sriram Rajagopal

IPC: A61K31/513 ,  C07D239/42 ,  A61K31/505

CPC classification number: C07D239/38 ,  C07D239/46 ,  C07D239/47 ,  C07D239/48 ,  C07D401/04

Abstract: The present invention relates to novel compounds of the general formula (I), 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 relates to novel pyrimidine carboxamides of the general formula (I). Also included is a method of prophylaxis or treatment of a pain disorder, immunological diseases, inflammation, 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 in a mammal comprising administering an effective amount of a compound of formula (I) as described above.

Abstract translation: 本发明涉及通式（I）的新化合物，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，它们的水合物，它们的溶剂化物，其药学上可接受的盐和组合物，其代谢物和前药。 本发明更具体地涉及通式（I）的新型嘧啶甲酰胺。 还包括预防或治疗疼痛障碍，免疫疾病，炎症，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 败血症 败血性休克 中毒性休克综合征; 发热和由于哺乳动物感染引起的肌痛，包括给予有效量的如上所述的式（I）化合物。

公开(公告)号：US20110269753A1

公开(公告)日：2011-11-03

申请号：US13143480

申请日：2010-01-21

Applicant: Gopalan Balasubramanian ,  Sukunath Narayanan ,  Ganapavarapu Veera Raghava Sharma ,  Lavanya Andiappan ,  Shridhar Narayanan ,  Sanjeev Saxena ,  Sridharan Rajagopal ,  Santosh Lolaknath Vishwakarma ,  Saravanan Thirunavukkarasu

Inventor： Gopalan Balasubramanian ,  Sukunath Narayanan ,  Ganapavarapu Veera Raghava Sharma ,  Lavanya Andiappan ,  Shridhar Narayanan ,  Sanjeev Saxena ,  Sridharan Rajagopal ,  Santosh Lolaknath Vishwakarma ,  Saravanan Thirunavukkarasu

IPC: A61K31/4439 ,  C07D407/10 ,  C07D403/14 ,  C07D405/14 ,  C07D413/10 ,  C07D413/14 ,  C07D498/04 ,  C07D498/14 ,  A61K31/427 ,  A61K31/506 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/422 ,  A61K31/423 ,  A61K31/437 ,  A61P29/00 ,  A61P37/00 ,  A61P11/06 ,  A61P11/00 ,  A61P11/08 ,  A61P17/00 ,  A61P27/14 ,  A61P17/06 ,  A61P1/04 ,  A61P1/00 ,  A61P27/02 ,  A61P19/04 ,  C07D417/14

CPC classification number: C07D413/04 ,  C07D417/04 ,  C07D417/14

Abstract: Compounds of the formula (I), their derivatives, analogs, tautomeric forms, regioisomers, stereoisomers, polymorphs, solvates, intermediates, pharmaceutically acceptable salts, pharmaceutical compositions, N-oxides, metabolites and prodrugs thereof. These compounds are phosphodiesterase type 4 (PDE4) inhibitors. They are useful in the treatment of a variety of allergic or inflammatory diseases including asthma, COPD, chronic bronchitis, atopic dermatitis, allergic rhinitis, allergic conjunctivitis, vernal conjunctivitis, psoriasis, rheumatoid arthritis, ulcerative colitis, Crohn's disease, uveitis, NASH and lupus.

Abstract translation: 式（I）化合物，其衍生物，类似物，互变异构体，区域异构体，立体异构体，多晶型物，溶剂合物，中间体，药学上可接受的盐，药物组合物，N-氧化物，代谢物和前药。 这些化合物是磷酸二酯酶4型（PDE4）抑制剂。 它们可用于治疗各种过敏或炎性疾病，包括哮喘，COPD，慢性支气管炎，特应性皮炎，过敏性鼻炎，过敏性结膜炎，春季结膜炎，牛皮癣，类风湿性关节炎，溃疡性结肠炎，克罗恩病，葡萄膜炎，NASH和狼疮 。

公开(公告)号：US07786142B2

公开(公告)日：2010-08-31

申请号：US11546299

申请日：2006-10-12

Applicant: 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

Inventor： 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: A61K31/4468 ,  A61K31/403 ,  C07D405/14 ,  C07D209/88

CPC classification number: C07D209/88 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D417/12

Abstract: 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

Abstract translation: 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：US20080221103A1

公开(公告)日：2008-09-11

申请号：US12073635

申请日：2008-03-07

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

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

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

CPC classification number: C07D239/24 ,  C07D413/14

Abstract: 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).

Abstract translation: 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：US07317014B2

公开(公告)日：2008-01-08

申请号：US10469647

申请日：2003-07-21

Applicant: Shiv Kumar Agarwal ,  Ravikumar Tadiparthi ,  Pawan Aggarwal ,  Savithiri Shivakumar

Inventor： Shiv Kumar Agarwal ,  Ravikumar Tadiparthi ,  Pawan Aggarwal ,  Savithiri Shivakumar

IPC: C07D239/30 ,  C07D239/48 ,  A61K31/505

CPC classification number: C07D239/30 ,  C07D239/36 ,  C07D239/38 ,  C07D239/42 ,  C07D239/47 ,  C07D239/48 ,  C07D239/56

Abstract: The present invention relates to novel derivatives of the general formula (I), their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their hydrates, their solvates, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them. The present invention more particularly provides novel pyrimidine derivatives of the general formula (I)

Abstract translation: 本发明涉及通式（I）的新衍生物，其衍生物，其类似物，其互变异构形式，它们的立体异构体，其多晶型物，它们的水合物，它们的溶剂化物，其药学上可接受的盐和含有它们的药学上可接受的组合物。 本发明更具体地提供了通式（I）的新型嘧啶衍生物，

公开(公告)号：US20070111998A1

公开(公告)日：2007-05-17

申请号：US11546299

申请日：2006-10-12

Applicant: Siripragada Rao ,  Akella Satya Srinivas ,  Shikha Rani ,  Gaddam Reddy ,  Sriram Rajagopal ,  Uma Ramachandran ,  Duddu Sharada ,  Rajagopalan Nirmala ,  Velaiah Sivasudar ,  Lakshmanan Manikandan ,  Ramachandran Balaji

Inventor： Siripragada Rao ,  Akella Satya Srinivas ,  Shikha Rani ,  Gaddam Reddy ,  Sriram Rajagopal ,  Uma Ramachandran ,  Duddu Sharada ,  Rajagopalan Nirmala ,  Velaiah Sivasudar ,  Lakshmanan Manikandan ,  Ramachandran Balaji

IPC: A61K31/541 ,  A61K31/5377 ,  A61K31/496 ,  A61K31/454 ,  A61K31/4439 ,  A61K31/427 ,  A61K31/416 ,  A61K31/403 ,  C07D417/02 ,  C07D403/02 ,  C07D413/02

CPC classification number: C07D209/88 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D417/12

Abstract: 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.

Abstract translation: 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：US07759350B2

公开(公告)日：2010-07-20

申请号：US11516549

申请日：2006-09-07

Applicant: Ravikumar Tadipartiii ,  Venkatesan Parameswaran ,  Rajib Barik ,  Gaddam Om Reddy ,  Pawan Aggarwal ,  Sappanimuthu Thirunavukkarasu ,  Sriram Rajagopal

Inventor： Ravikumar Tadipartiii ,  Venkatesan Parameswaran ,  Rajib Barik ,  Gaddam Om Reddy ,  Pawan Aggarwal ,  Sappanimuthu Thirunavukkarasu ,  Sriram Rajagopal

IPC: C07D239/28 ,  A61K31/505

CPC classification number: C07D239/38 ,  C07D239/46 ,  C07D239/47 ,  C07D239/48 ,  C07D401/04

Abstract: The present invention relates to novel compounds of the general formula (I), 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 relates to novel pyrimidine carboxamides of the general formula (I). Also included is a method of prophylaxis or treatment of a pain disorder, immunological diseases, inflammation, 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 in a mammal comprising administering an effective amount of a compound of formula (I) as described above.

Abstract translation: 本发明涉及通式（I）的新化合物，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，它们的水合物，它们的溶剂化物，其药学上可接受的盐和组合物，其代谢物和前药。 本发明更具体地涉及通式（I）的新型嘧啶甲酰胺。 还包括预防或治疗疼痛障碍，免疫疾病，炎症，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 败血症 败血性休克 中毒性休克综合征; 发热和由于哺乳动物感染引起的肌痛，包括给予有效量的如上所述的式（I）化合物。

公开(公告)号：US20090069313A1

公开(公告)日：2009-03-12

申请号：US11896902

申请日：2007-09-06

Applicant: Debendranath Dey ,  Gajendra Singh ,  Partha Neogi ,  Uma Ramachandran ,  Chithra Santhanagopalan

Inventor： Debendranath Dey ,  Gajendra Singh ,  Partha Neogi ,  Uma Ramachandran ,  Chithra Santhanagopalan

IPC: A61K31/5377 ,  C07D277/16 ,  A61K31/426 ,  C07D209/34 ,  A61P25/24 ,  A61P25/32 ,  A61P25/08 ,  A61P25/00 ,  A61P25/34 ,  A61P25/28 ,  A61K31/404 ,  C07D413/12 ,  A61K31/422

CPC classification number: C07D277/36 ,  C07D209/34 ,  C07D277/34 ,  C07D413/12 ,  C07D417/12

Abstract: The present invention provides a new medical use for the compounds of the formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts and compositions, metabolites and prodrugs thereof, as MAO-A inhibitors. Also included is a method for prophylaxis and treatment of mental disorders such as depression, in a mammal, comprising administering an effective amount of a compound of formula (I). These compounds are also effective in treating a disease, condition or disorder such as weight loss, obesity, bulimia, depression, bipolar disorders, psychoses, schizophrenia, behaviors, alcoholism, tobacco abuse, memory loss, Alzheimer's disease, dementia of aging, seizure disorders, epilepsy, attention deficit disorder, and Parkinson's disease, which is modulated by a cannabinoid receptor antagonist.

Abstract translation: 本发明提供了作为MAO-A抑制剂的式（I）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，其代谢物和前药的新医学用途 。 还包括在哺乳动物中预防和治疗精神障碍如抑郁症的方法，包括施用有效量的式（I）化合物。 这些化合物在治疗疾病，病症或病症如体重减轻，肥胖，贪食症，抑郁症，双相性精神障碍，精神病，精神分裂症，行为，酒精中毒，吸烟，记忆丧失，阿尔茨海默病，老年痴呆，癫痫发作障碍 ，癫痫，注意力缺陷障碍和由大麻素受体拮抗剂调节的帕金森病。