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1. 发明申请

WO2008110891A2 NEW HETEROCYCLIC COMPOUNDS 审中-公开
标题翻译：新的杂环化合物
公开(公告)号：WO2008110891A2
公开(公告)日：2008-09-18
申请号：PCT/IB2008/000536
申请日：2008-03-07
申请人： ORCHID RESEARCH LABORATORIES LIMITED, , SHARMA, Ganapavarapu, Veera, Raghava , REDDY, Gaddam, Om , RAJAGOPAL, Sriram , RAMACHANDRAN, Uma , NARAYANAN, Sukunath , PICHIKA, Nagalakshmi , NEMMARA VISWANATHAN, Venkatesh , ANDIAPPAN, Lavanya , THIRUNAVUKKARASU, Saravanan
发明人： SHARMA, Ganapavarapu, Veera, Raghava , REDDY, Gaddam, Om , RAJAGOPAL, Sriram , RAMACHANDRAN, Uma , NARAYANAN, Sukunath , PICHIKA, Nagalakshmi , NEMMARA VISWANATHAN, Venkatesh , ANDIAPPAN, Lavanya , THIRUNAVUKKARASU, Saravanan
IPC分类号： C07D401/12
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 R 1 , R 2 , R 3 , R 4 and R 5 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通过在患者中给予一种或多种TNF-α，血栓烷合成酶，5-LOX和PDE4抑制剂来治疗各种疾病和病症的式（I）的杂环化合物。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 uveititis; 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; 溃疡性结肠炎过敏性反应; 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由于HIV-1介导的感染和疾病引起的发热和肌痛; 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。

2. 发明申请

WO2007007161A2 NOVEL BIO-ACTIVE DERIVATIVES 审中-公开
标题翻译：新型生物活性衍生物
公开(公告)号：WO2007007161A2
公开(公告)日：2007-01-18
申请号：PCT/IB2006/001895
申请日：2006-07-10
申请人： ORCHID RESEARCH LABORATORIES LIMITED , TADIPARTHI, Ravikumar , SHARMA, Ganapavarapu, Veera, Raghava , NARAYANAN, Sukunath , PARAMESWARAN, Venkatesan , REDDY, Gaddam, Om , RAJAGOPAL, Sriram , NATARAJAN, Manikandan , KOPPOLU, Kesavan
发明人： TADIPARTHI, Ravikumar , SHARMA, Ganapavarapu, Veera, Raghava , NARAYANAN, Sukunath , PARAMESWARAN, Venkatesan , REDDY, Gaddam, Om , RAJAGOPAL, Sriram , NATARAJAN, Manikandan , KOPPOLU, Kesavan
IPC分类号： C07D239/54 , A61K31/513
CPC分类号： C07D239/54 , C07D401/06 , C07D401/12 , C07D403/06 , C07D405/06 , C07D413/06 , C07D417/12
摘要： 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 pharmaceutically acceptable compositions containing them. The present invention more particularly provides novel compounds of the general formula (I).
摘要翻译：本发明涉及通式（I）的新化合物，其衍生物，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，它们的水合物，它们的溶剂化物，它们的药学上可接受的盐和含有它们的药学可接受组合物本发明更具体地提供了通式（I）的新型化合物。

3. 发明申请

WO2008087514A3 HDAC INHIBITORS 审中-公开
公开(公告)号：WO2008087514A3
公开(公告)日：2008-07-24
申请号：PCT/IB2008/000045
申请日：2008-01-10
申请人： ORCHID RESEARCH LABORATORIES LIMITED , KACHHADIA, Virendra , PUNTHALIR, Narayanaswamy , PONPANDIAN, Thanasekaran , DAIVASIGAMANI, Prabhu , SRINIVAS, Akella, Satya, Visweswara , RAMACHANDRAN, Uma , RAJAGOPAL, Sriram , REDDY, Gaddam, Om , RAJAGOPAL, Sridahran , KEERI, Abdul, Raheem
发明人： KACHHADIA, Virendra , PUNTHALIR, Narayanaswamy , PONPANDIAN, Thanasekaran , DAIVASIGAMANI, Prabhu , SRINIVAS, Akella, Satya, Visweswara , RAMACHANDRAN, Uma , RAJAGOPAL, Sriram , REDDY, Gaddam, Om , RAJAGOPAL, Sridahran , KEERI, Abdul, Raheem
IPC分类号： C07D417/12 , C07D417/14 , C07D409/12 , C07D405/12 , C07D403/12 , C07D241/04 , C07C233/01 , C07C233/16 , C07C233/64
摘要： Novel compounds of the formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts and compositions, metabolites and prodrugs thereof are described. These novel compounds can inhibit HDACs and are useful as a therapeutic or ameliorating agent for diseases that are involved in cellular growth such as malignant tumors, autoimmune diseases, skin diseases, infections, inflammation, cancer, psoriasis, proliferative conditions and conditions mediated by HDAC.

4. 发明申请

WO2007042912A3 HETEROCYCLIC COMPOUNDS AS PSTAT3/IL-6 INHIBITORS 审中-公开
公开(公告)号：WO2007042912A3
公开(公告)日：2007-04-19
申请号：PCT/IB2006/002829
申请日：2006-10-11
申请人： ORCHID RESEARCH LABORATORIES LIMITED , RAO, Siripragada, Mahender , SRINIVAS, Akella, Satya, Surya, Visweswara , RANI, Shikha , REDDY, Gaddam, Om , RAJAGOPAL, Sriram , RAMACHANDRAN, Uma , SHARADA, Duddu, Savaraiah , NIRMALA, Rajagopalan , SIVASUDAR, Velaiah , MANIKANDAN, Lakshmanan , BALAJI, Ramachandran
发明人： RAO, Siripragada, Mahender , SRINIVAS, Akella, Satya, Surya, Visweswara , RANI, Shikha , REDDY, Gaddam, Om , RAJAGOPAL, Sriram , RAMACHANDRAN, Uma , SHARADA, Duddu, Savaraiah , NIRMALA, Rajagopalan , SIVASUDAR, Velaiah , MANIKANDAN, Lakshmanan , BALAJI, Ramachandran
IPC分类号： C07D209/88 , C07D495/04 , C07D403/12 , C07D417/12 , C07D405/14 , C07D409/12 , C07D401/12 , A61K31/403 , A61P35/00
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.

5. 发明申请

WO2007017728A3 NOVEL HETEROCYCLIC COMPOUNDS 审中-公开
公开(公告)号：WO2007017728A3
公开(公告)日：2007-02-15
申请号：PCT/IB2006/002139
申请日：2006-08-04
申请人： ORCHID RESEARCH LABORATORIES LIMITED , SRINIVAS, Akella, Satya, Surya, Visweswara , MATHIYAZHAGAN, Kasinathan , SHARADA, Duddu, Savaraiah , PONPANDIAN, Thanasekaran , REVATHY, Kulasekharan , REDDY, Gaddam, Om , KAMARAJ, Mani , RAJAGOPAL, Sriram
发明人： SRINIVAS, Akella, Satya, Surya, Visweswara , MATHIYAZHAGAN, Kasinathan , SHARADA, Duddu, Savaraiah , PONPANDIAN, Thanasekaran , REVATHY, Kulasekharan , REDDY, Gaddam, Om , KAMARAJ, Mani , RAJAGOPAL, Sriram
IPC分类号： C07D417/12 , C07C271/10 , C07D277/38 , C07D333/16
摘要： The present invention relates to novel compounds of the general formula (I), their derivatives, their analogs, their stereoisomers, their pharmaceutically acceptable salts and compositions. The present invention more particularly provides novel heterocyclic compounds of the general formula (I).

6. 发明申请

WO2007096740A2 NOVEL CEPHALOSPORINS 审中-公开
标题翻译：新型头孢菌素
公开(公告)号：WO2007096740A2
公开(公告)日：2007-08-30
申请号：PCT/IB2007/000403
申请日：2007-02-20
申请人： ORCHID RESEARCH LABORATORIES LIMITED , RAMACHANDRAN, Uma , REDDY, Gaddam, Om , TADIPARTHI, Ravikumar , THERATIPALLY, Prabhakar , VENKATESHWARLU, Jakkala , SUBRAMANIAN, Santhosh
发明人： RAMACHANDRAN, Uma , REDDY, Gaddam, Om , TADIPARTHI, Ravikumar , THERATIPALLY, Prabhakar , VENKATESHWARLU, Jakkala , SUBRAMANIAN, Santhosh
IPC分类号： C07D501/24 , A61K31/547
CPC分类号： C07D501/46
摘要： The present invention relates to novel 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 cephalosporin antibiotics of the general formula (I). Also included is a method for treatment of infectious diseases 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，代谢物和前药。本发明更具体地提供了通式（I）的新型头孢菌素抗生素。还包括治疗哺乳动物感染性疾病的方法，包括给予有效量的如上所述的式（I）化合物。

7. 发明申请

WO2007054776A9 STILBENE LIKE COMPOUNDS AS NOVEL HDAC INHIBITORS 审中-公开
公开(公告)号：WO2007054776A9
公开(公告)日：2007-05-18
申请号：PCT/IB2006/003114
申请日：2006-11-06
申请人： ORCHID RESEARCH LABORATORIES LIMITED , SRINIVAS, Akella, Satya, Surya, Visweswara , BALAN, Urkalan, Kaveri , PUNTHALIR, Narayana, Swamy , VELMURUGAN, Rama, Swamy , RAJAGOPAL, Sriram , REDDY, Gaddam, Om , KACHHADIA, Virendra
发明人： SRINIVAS, Akella, Satya, Surya, Visweswara , BALAN, Urkalan, Kaveri , PUNTHALIR, Narayana, Swamy , VELMURUGAN, Rama, Swamy , RAJAGOPAL, Sriram , REDDY, Gaddam, Om , KACHHADIA, Virendra
IPC分类号： C07C235/72 , C07C233/46 , C07C235/34 , C07D277/30 , C07D333/24 , A61K31/165
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.

8. 发明申请

WO2007113644A2 NEW HDAC INHIBITORS 审中-公开
标题翻译：新型HDAC抑制剂
公开(公告)号：WO2007113644A2
公开(公告)日：2007-10-11
申请号：PCT/IB2007/000853
申请日：2007-04-03
申请人： ORCHID RESEARCH LABORATORIES LIMITED , SRINIVAS, Akella, Satya, Surya, Visweswara , KACHHADIA, Virendra , MATHIYAZHAGAN, Kasinathan , THARA, Sathya, Narayana , MANIKANDAN, Lakshmanan , RAJAGOPAL, Sriram , REDDY, Gaddam, Om
发明人： SRINIVAS, Akella, Satya, Surya, Visweswara , KACHHADIA, Virendra , MATHIYAZHAGAN, Kasinathan , THARA, Sathya, Narayana , MANIKANDAN, Lakshmanan , RAJAGOPAL, Sriram , REDDY, Gaddam, Om
IPC分类号： C07C233/01 , C07C257/06 , C07C327/40 , C07C259/06 , C07C327/22 , C07D295/15
CPC分类号： C07D277/82 , C07D307/68
摘要： The present invention relates to novel compounds of the general formula (I), having histone deacetylase (HDAC) inhibiting enzymatic activity, 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 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：本发明涉及具有抑制酶活性的组蛋白脱乙酰酶（HDAC），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，代谢物和前药的通式（I）的新型化合物它们。本发明更具体地提供了通式（I）的新型化合物。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。

9. 发明申请

WO2007045962A2 NOVEL HDAC INHIBITORS 审中-公开
标题翻译：新型HDAC抑制剂
公开(公告)号：WO2007045962A2
公开(公告)日：2007-04-26
申请号：PCT/IB2006/002890
申请日：2006-10-17
申请人： ORCHID RESEARCH LABORATORIES LIMITED , SRINIVAS, Akella, Satya, Surya, Visweswara , NARASIMHAN, Kilambi , MANIKANDAN, Lakshmanan , RAJAGOPAL, Sriram , SELVAKUMAR, Thangapazham , REDDY, Gaddam, Om
发明人： SRINIVAS, Akella, Satya, Surya, Visweswara , NARASIMHAN, Kilambi , MANIKANDAN, Lakshmanan , RAJAGOPAL, Sriram , SELVAKUMAR, Thangapazham , REDDY, Gaddam, Om
IPC分类号： C07D241/04
CPC分类号： C07D277/46 , C07D277/82 , C07D295/185
摘要： Abstract The present invention relates to novel compounds of the general formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts and compositions. The present invention more particularly provides novel HDAC inhibitors of the general formula (1). 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 compound of formula (I) as described above.
摘要翻译：摘要本发明涉及通式（I）的新化合物，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。本发明更具体地提供了通式（1）的新型HDAC抑制剂。还包括在哺乳动物中治疗癌症，牛皮癣，增殖性病症和HDAC介导的病症的方法，包括给予有效量的如上所述的式（I）化合物。

10. 发明申请

WO2007031829A2 NOVEL PYRIMIDINE CARBOXAMIDES 审中-公开
标题翻译：新的嘧啶甲酰胺
公开(公告)号：WO2007031829A2
公开(公告)日：2007-03-22
申请号：PCT/IB2006/002461
申请日：2006-09-07
申请人： ORCHID RESEARCH LABORATORIES LIMITED , TADIPARTHI, Ravikumar , AGGARWAL, Pawan , PARAMESWARAN, Venkatesan , THIRUNAVUKKARASU, Sappanimuthu , BARIK, Rajib , RAJAGOPAL, Sriram , REDDY, Gaddam, Om
发明人： TADIPARTHI, Ravikumar , AGGARWAL, Pawan , PARAMESWARAN, Venkatesan , THIRUNAVUKKARASU, Sappanimuthu , BARIK, Rajib , RAJAGOPAL, Sriram , REDDY, Gaddam, Om
IPC分类号： C07D239/28
CPC分类号： C07D239/38 , C07D239/46 , C07D239/47 , C07D239/48 , C07D401/04
摘要： 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.
摘要翻译：本发明涉及通式（I）的新化合物，其衍生物，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，它们的水合物，它们的溶剂化物，它们的药学上可接受的盐和组合物，它们的代谢物和前药。本发明更具体地涉及通式（I）的新型嘧啶甲酰胺。还包括预防或治疗疼痛病症，免疫性疾病，炎症，类风湿性关节炎的方法; 骨质疏松症; 多发性骨髓瘤; uveititis; 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; 类风湿性脊椎炎; 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; 过敏性反应; 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; 感染性休克; 中毒性休克综合症发热和由于哺乳动物感染引起的肌痛，包括施用有效量的如上所述的式（I）化合物。

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