公开(公告)号：WO2009095773A8

公开(公告)日：2010-01-07

申请号：PCT/IB2009000157

申请日：2009-01-30

Applicant: ORCHID RES LAB LTD ,  SRINIVAS VISWESWARA AKELLA SATYA SURYA ,  TADIPARTHI RAVIKUMAR ,  SHARMA GANAPAVARAPU VEERA RAGHAVA ,  SAPPANIMUTHU THIRUNAVUKKARASU ,  BHAKIARAJ DURAIRAJ PETER ,  KACHHADIA VIRENDRA ,  NARASIMHAN KILAMBI ,  THARA SATHYA NARAYANA ,  RAJAGOPAL SRIRAM ,  NARAYANAN SUKUNATH ,  PARAMESWARAN VENKATESAN ,  JANARTHANAM VENKATESAN ,  NARAYANAM MARUTHIKUMAR ,  GADDE SATHYANARAYANA ,  RAMACHANDRAN UMA ,  BALASUBRAMANIAN GOPALAN ,  SURENDRAN NARAYANAN ,  NARAYANAN SHRIDHAR ,  VISHWAKARMA LOLAKNATH SANTOSH ,  SAXENA SANJEEV

Inventor： SRINIVAS VISWESWARA AKELLA SATYA SURYA ,  TADIPARTHI RAVIKUMAR ,  SHARMA GANAPAVARAPU VEERA RAGHAVA ,  SAPPANIMUTHU THIRUNAVUKKARASU ,  BHAKIARAJ DURAIRAJ PETER ,  KACHHADIA VIRENDRA ,  NARASIMHAN KILAMBI ,  THARA SATHYA NARAYANA ,  RAJAGOPAL SRIRAM ,  NARAYANAN SUKUNATH ,  PARAMESWARAN VENKATESAN ,  JANARTHANAM VENKATESAN ,  NARAYANAM MARUTHIKUMAR ,  GADDE SATHYANARAYANA ,  RAMACHANDRAN UMA ,  BALASUBRAMANIAN GOPALAN ,  SURENDRAN NARAYANAN ,  NARAYANAN SHRIDHAR ,  VISHWAKARMA LOLAKNATH SANTOSH ,  SAXENA SANJEEV ,  REDDY GADDAM OM

IPC: C07D403/04 ,  C07D239/26 ,  C07D401/04

CPC classification number: C07D239/42 ,  A61K31/5377 ,  C07D265/28 ,  C07D401/04

Abstract: 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.

Abstract translation: 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，溶剂化物，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性疾病，炎症，疼痛病症，类风湿性关节炎; 骨质疏松症; 多发性骨髓瘤; uveititis; 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; 类风湿性脊椎炎; 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; 过敏性反应; 接触性皮炎; 肌肉退化; 哮喘; 慢性阻塞性肺病; 骨吸收疾病; 多发性硬化症; 败血症; 感染性休克; 中毒性休克综合症和发烧。 更具体地说，这些化合物可用作PDE4抑制剂并可用于治疗PDE4介导的疾病。

公开(公告)号：WO2007083182A2

公开(公告)日：2007-07-26

申请号：PCT/IB2006/003468

申请日：2006-12-01

Applicant: ORCHID RESEARCH LABORATORIES LIMITED ,  SRINIVAS, Visweswara, Akella, Staya, Surya ,  TADIPARTHI, Ravikumar ,  SHARMA, Ganapavarapu, Veera, Raghava ,  THIRUNAVUKKARASU, Sappanimuthu ,  BHAKIARAJ, Durairaj, Peter ,  KACHHADIA, Virendra ,  NARSIMHAN, Kilambi ,  THARA, Sathya, Narayana ,  RAJAGOPAL, Sriram ,  REEDY, Gaddam, Om ,  NARAYANAN, Sukunath ,  PARAMESWARAN, Venkatesan ,  JANARTHANAM, Venkatesan

Inventor： SRINIVAS, Visweswara, Akella, Staya, Surya ,  TADIPARTHI, Ravikumar ,  SHARMA, Ganapavarapu, Veera, Raghava ,  THIRUNAVUKKARASU, Sappanimuthu ,  BHAKIARAJ, Durairaj, Peter ,  KACHHADIA, Virendra ,  NARSIMHAN, Kilambi ,  THARA, Sathya, Narayana ,  RAJAGOPAL, Sriram ,  REEDY, Gaddam, Om ,  NARAYANAN, Sukunath ,  PARAMESWARAN, Venkatesan ,  JANARTHANAM, Venkatesan

IPC: C07D233/96

CPC classification number: C07D239/42 ,  C07D213/30 ,  C07D239/32 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D407/12 ,  C07D409/12 ,  C07D409/14 ,  C07D413/04 ,  C07D417/12 ,  C07D417/14

Abstract: The present invention relates to novel 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. The present invention more particularly provides novel hetereocycles of the general formula (I). Also included is a method of treatment of 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 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，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，溶剂化物，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新的通式（I）的杂环。 还包括治疗免疫性疾病，炎症，疼痛病症，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。

公开(公告)号：WO2009095773A3

公开(公告)日：2010-04-22

申请号：PCT/IB2009000157

申请日：2009-01-30

Applicant: ORCHID RES LAB LTD ,  SRINIVAS VISWESWARA AKELLA SATYA SURYA ,  TADIPARTHI RAVIKUMAR ,  SHARMA GANAPAVARAPU VEERA RAGHAVA ,  SAPPANIMUTHU THIRUNAVUKKARASU ,  BHAKIARAJ DURAIRAJ PETER ,  KACHHADIA VIRENDRA ,  NARASIMHAN KILAMBI ,  THARA SATHYA NARAYANA ,  RAJAGOPAL SRIRAM ,  NARAYANAN SUKUNATH ,  PARAMESWARAN VENKATESAN ,  JANARTHANAM VENKATESAN ,  NARAYANAM MARUTHIKUMAR ,  GADDE SATHYANARAYANA ,  RAMACHANDRAN UMA ,  BALASUBRAMANIAN GOPALAN ,  SURENDRAN NARAYANAN ,  NARAYANAN SHRIDHAR ,  VISHWAKARMA LOLAKNATH SANTOSH ,  SAXENA SANJEEV

Inventor： SRINIVAS VISWESWARA AKELLA SATYA SURYA ,  TADIPARTHI RAVIKUMAR ,  SHARMA GANAPAVARAPU VEERA RAGH ,  SAPPANIMUTHU THIRUNAVUKKARASU ,  BHAKIARAJ DURAIRAJ PETER ,  KACHHADIA VIRENDRA ,  NARASIMHAN KILAMBI ,  THARA SATHYA NARAYANA ,  RAJAGOPAL SRIRAM ,  NARAYANAN SUKUNATH ,  PARAMESWARAN VENKATESAN ,  JANARTHANAM VENKATESAN ,  NARAYANAM MARUTHIKUMAR ,  GADDE SATHYANARAYANA ,  RAMACHANDRAN UMA ,  BALASUBRAMANIAN GOPALAN ,  SURENDRAN NARAYANAN ,  NARAYANAN SHRIDHAR ,  VISHWAKARMA LOLAKNATH SANTOSH ,  SAXENA SANJEEV ,  REDDY GADDAM OM

IPC: C07D239/42 ,  A61K31/505 ,  C07D213/30 ,  C07D239/32 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12

CPC classification number: C07D239/42 ,  A61K31/5377 ,  C07D265/28 ,  C07D401/04

Abstract: 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.

Abstract translation: 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，溶剂化物，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 uveititis; 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; 类风湿性脊椎炎; 痛风性关节炎 炎性肠病; 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; 肌肉变性 哮喘; 慢性阻塞性肺病; 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。 更具体地说，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：WO2007083182A3

公开(公告)日：2007-11-15

申请号：PCT/IB2006003468

申请日：2006-12-01

Applicant: ORCHID RES LAB LTD ,  SRINIVAS VISWESWARA AKELLA STA ,  TADIPARTHI RAVIKUMAR ,  SHARMA GANAPAVARAPU VEERA RAGH ,  THIRUNAVUKKARASU SAPPANIMUTHU ,  BHAKIARAJ DURAIRAJ PETER ,  KACHHADIA VIRENDRA ,  NARSIMHAN KILAMBI ,  THARA SATHYA NARAYANA ,  RAJAGOPAL SRIRAM ,  REEDY GADDAM OM ,  NARAYANAN SUKUNATH ,  PARAMESWARAN VENKATESAN ,  JANARTHANAM VENKATESAN

Inventor： SRINIVAS VISWESWARA AKELLA STA ,  TADIPARTHI RAVIKUMAR ,  SHARMA GANAPAVARAPU VEERA RAGH ,  THIRUNAVUKKARASU SAPPANIMUTHU ,  BHAKIARAJ DURAIRAJ PETER ,  KACHHADIA VIRENDRA ,  NARSIMHAN KILAMBI ,  THARA SATHYA NARAYANA ,  RAJAGOPAL SRIRAM ,  REEDY GADDAM OM ,  NARAYANAN SUKUNATH ,  PARAMESWARAN VENKATESAN ,  JANARTHANAM VENKATESAN

IPC: C07D233/96 ,  A61K31/505

CPC classification number: C07D239/42 ,  C07D213/30 ,  C07D239/32 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D407/12 ,  C07D409/12 ,  C07D409/14 ,  C07D413/04 ,  C07D417/12 ,  C07D417/14

Abstract: The present invention relates to novel 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. The present invention more particularly provides novel hetereocycles of the general formula (I). Also included is a method of treatment of 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 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，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，溶剂化物，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）的新颖的杂环。 还包括治疗免疫疾病，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; 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：WO2007031829A3

公开(公告)日：2007-11-08

申请号：PCT/IB2006002461

申请日：2006-09-07

Applicant: ORCHID RES LAB LTD ,  TADIPARTHI RAVIKUMAR ,  AGGARWAL PAWAN ,  PARAMESWARAN VENKATESAN ,  THIRUNAVUKKARASU SAPPANIMUTHU ,  BARIK RAJIB ,  RAJAGOPAL SRIRAM ,  REDDY GADDAM OM

Inventor： TADIPARTHI RAVIKUMAR ,  AGGARWAL PAWAN ,  PARAMESWARAN VENKATESAN ,  THIRUNAVUKKARASU SAPPANIMUTHU ,  BARIK RAJIB ,  RAJAGOPAL SRIRAM ,  REDDY GADDAM OM

IPC: C07D239/28

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，其水合物，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 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 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：WO2009095773A2

公开(公告)日：2009-08-06

申请号：PCT/IB2009/000157

申请日：2009-01-30

Applicant: ORCHID RESEARCH LABORATORIES LIMITED ,  ORCHID RESEARCH LABORATORIES LIMITED ,  SRINIVAS, Visweswara, Akella, Satya, Surya ,  TADIPARTHI, Ravikumar ,  SHARMA, Ganapavarapu, Veera, Raghava ,  SAPPANIMUTHU, Thirunavukkarasu ,  BHAKIARAJ, Durairaj, Peter ,  KACHHADIA, Virendra ,  NARASIMHAN, Kilambi ,  THARA, Sathya, Narayana ,  RAJAGOPAL, Sriram ,  NARAYANAN, Sukunath ,  PARAMESWARAN, Venkatesan ,  JANARTHANAM, Venkatesan ,  NARAYANAM, Maruthikumar ,  GADDE, Sathyanarayana ,  RAMACHANDRAN, Uma ,  BALASUBRAMANIAN, Gopalan ,  SURENDRAN, Narayanan ,  NARAYANAN, Shridhar ,  VISHWAKARMA, Lolaknath, Santosh ,  SAXENA, Sanjeev

Inventor： SRINIVAS, Visweswara, Akella, Satya, Surya ,  TADIPARTHI, Ravikumar ,  SHARMA, Ganapavarapu, Veera, Raghava ,  SAPPANIMUTHU, Thirunavukkarasu ,  BHAKIARAJ, Durairaj, Peter ,  KACHHADIA, Virendra ,  NARASIMHAN, Kilambi ,  THARA, Sathya, Narayana ,  RAJAGOPAL, Sriram ,  NARAYANAN, Sukunath ,  PARAMESWARAN, Venkatesan ,  JANARTHANAM, Venkatesan ,  NARAYANAM, Maruthikumar ,  GADDE, Sathyanarayana ,  RAMACHANDRAN, Uma ,  BALASUBRAMANIAN, Gopalan ,  SURENDRAN, Narayanan ,  NARAYANAN, Shridhar ,  VISHWAKARMA, Lolaknath, Santosh ,  SAXENA, Sanjeev

IPC: C07D403/04 ,  C07D401/04 ,  C07D239/26

CPC classification number: C07D239/42 ,  A61K31/5377 ,  C07D265/28 ,  C07D401/04

Abstract: 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.

Abstract translation: 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性疾病，炎症，疼痛障碍，类风湿性关节炎; 骨质疏松症; 多发性骨髓瘤 uveititis; 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 过敏性反应; 接触性皮炎; 肌肉退化; 哮喘; 慢性阻塞性肺病; 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：WO2006129181A3

公开(公告)日：2007-12-27

申请号：PCT/IB2006001448

申请日：2006-06-02

Applicant: ORCHID RES LAB LTD ,  TADIPARTHI RAVIKUMAR ,  AGGARWAL PAWAN ,  REDDY GADDAM OM ,  PARAMESWARAN VENKATESAN ,  RAJAGOPAL SRIRAM ,  RAGHUVEERASWAMINATHAN SANKARAN

Inventor： TADIPARTHI RAVIKUMAR ,  AGGARWAL PAWAN ,  REDDY GADDAM OM ,  PARAMESWARAN VENKATESAN ,  RAJAGOPAL SRIRAM ,  RAGHUVEERASWAMINATHAN SANKARAN

IPC: C07D239/47 ,  A61K31/513 ,  C07D239/48 ,  C07D401/04

CPC classification number: C07D239/56 ,  C07D239/47 ,  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 and their pharmaceutically acceptable salts and compositions. The present invention more particularly provides novel pyrimidones of the general formula (I).

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，其多晶型物及其药学上可接受的盐和组合物。 本发明更具体地提供通式（I）的新型嘧啶酮。

公开(公告)号：WO2007007161A3

公开(公告)日：2007-08-23

申请号：PCT/IB2006001895

申请日：2006-07-10

Applicant: ORCHID RES LAB LTD ,  TADIPARTHI RAVIKUMAR ,  SHARMA GANAPAVARAPU VEERA RAGH ,  NARAYANAN SUKUNATH ,  PARAMESWARAN VENKATESAN ,  REDDY GADDAM OM ,  RAJAGOPAL SRIRAM ,  NATARAJAN MANIKANDAN ,  KOPPOLU KESAVAN

Inventor： TADIPARTHI RAVIKUMAR ,  SHARMA GANAPAVARAPU VEERA RAGH ,  NARAYANAN SUKUNATH ,  PARAMESWARAN VENKATESAN ,  REDDY GADDAM OM ,  RAJAGOPAL SRIRAM ,  NATARAJAN MANIKANDAN ,  KOPPOLU KESAVAN

IPC: C07D239/54 ,  A61K31/513

CPC classification number: C07D239/54 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D405/06 ,  C07D413/06 ,  C07D417/12

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 pharmaceutically acceptable compositions containing them. The present invention more particularly provides novel compounds of the general formula (I).

Abstract translation: 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，它们的溶剂合物，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）的新化合物。

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

Applicant: ORCHID RESEARCH LABORATORIES LIMITED ,  TADIPARTHI, Ravikumar ,  AGGARWAL, Pawan ,  PARAMESWARAN, Venkatesan ,  THIRUNAVUKKARASU, Sappanimuthu ,  BARIK, Rajib ,  RAJAGOPAL, Sriram ,  REDDY, Gaddam, Om

Inventor： TADIPARTHI, Ravikumar ,  AGGARWAL, Pawan ,  PARAMESWARAN, Venkatesan ,  THIRUNAVUKKARASU, Sappanimuthu ,  BARIK, Rajib ,  RAJAGOPAL, Sriram ,  REDDY, Gaddam, Om

IPC: C07D239/28

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，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。

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

Applicant: ORCHID RESEARCH LABORATORIES LIMITED ,  TADIPARTHI, Ravikumar ,  SHARMA, Ganapavarapu, Veera, Raghava ,  NARAYANAN, Sukunath ,  PARAMESWARAN, Venkatesan ,  REDDY, Gaddam, Om ,  RAJAGOPAL, Sriram ,  NATARAJAN, Manikandan ,  KOPPOLU, Kesavan

Inventor： TADIPARTHI, Ravikumar ,  SHARMA, Ganapavarapu, Veera, Raghava ,  NARAYANAN, Sukunath ,  PARAMESWARAN, Venkatesan ,  REDDY, Gaddam, Om ,  RAJAGOPAL, Sriram ,  NATARAJAN, Manikandan ,  KOPPOLU, Kesavan

IPC: C07D239/54 ,  A61K31/513

CPC classification number: C07D239/54 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D405/06 ,  C07D413/06 ,  C07D417/12

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 pharmaceutically acceptable compositions containing them. The present invention more particularly provides novel compounds of the general formula (I).

Abstract translation: 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。