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12 条记录 (耗时 0.165 秒)

    Metabolites of tricyclic amides useful for inhibition of G-protein function and methods of treatment of proliferative diseases
    1.
    发明授权
    Metabolites of tricyclic amides useful for inhibition of G-protein function and methods of treatment of proliferative diseases 失效
    用于抑制G蛋白功能的三环酰胺的代谢物和治疗增殖性疾病的方法

    公开(公告)号：US07271174B2

    公开(公告)日：2007-09-18

    申请号：US10874556

    申请日：2004-06-23

    申请人： Swapan K. Chowdhury ,  Anima Ghosal ,  Robert M. Iannucci ,  Wenqing Feng ,  Tze-Ming Chan ,  Shmuel Zbaida ,  Kevin B. Alton ,  Ronald J. Doll ,  Keith P. Minor

    发明人： Swapan K. Chowdhury ,  Anima Ghosal ,  Robert M. Iannucci ,  Wenqing Feng ,  Tze-Ming Chan ,  Shmuel Zbaida ,  Kevin B. Alton ,  Ronald J. Doll ,  Keith P. Minor

    IPC分类号： C07D221/06 ,  A61K31/435

    CPC分类号： C07D401/14

    摘要： The present invention relates to metabolites of tricyclic amides, and structurally related compounds, represented by the structural formula (I): and pharmaceutically acceptable isomers, salts, solvates or esters of the compound of formula (I), wherein: R1 is selected from the group consisting of H and ═O; R2-R5 can be the same or different, each being independently selected from the group consisting of H, —OH, halide, —NH2 and ═O; and, the combination solid-dashed lines independently represent either single bonds or double bonds, wherein the number of combination solid-dashed lines that are double bonds is not greater than 2, and when, the double bonds are not adjacent, and when 0, one of R1-R5 is not H. Also disclosed are methods of treatment of proliferative diseases and methods for inhibiting the abnormal growth of cells, and for inhibiting farnesyl protein transferase using the novel compounds.

    摘要翻译： 本发明涉及由结构式（I）表示的三环酰胺的代谢物和结构相关的化合物：和式（I）化合物的药学上可接受的异构体，盐，溶剂化物或酯，其中：R 1 选自H和-O; R 2 -R 5可以相同或不同，各自独立地选自H，-OH，卤化物，-NH 2， SUB>和-O; 并且，组合虚线独立地表示单键或双键，其中双键的组合实线的数目不大于2，当双键不相邻时，当为0时， R 1〜R 5之一不是H.还公开了治疗增殖性疾病的方法和抑制细胞异常生长的方法，以及用于抑制法呢基蛋白转移酶 使用新型化合物。

    Metabolite of xanthine Phosphodiesterase 5 inhibitor and derivatives thereof useful for treatment of erectile dysfunction
    3.
    发明授权
    Metabolite of xanthine Phosphodiesterase 5 inhibitor and derivatives thereof useful for treatment of erectile dysfunction 失效
    黄嘌呤的代谢物磷酸二酯酶5抑制剂及其衍生物可用于治疗勃起功能障碍

    公开(公告)号：US07312223B2

    公开(公告)日：2007-12-25

    申请号：US10901574

    申请日：2004-07-29

    申请人： Anima Ghosal ,  Wei Tong ,  Swapan K. Chowdhury ,  Shmuel Zbaida ,  Mark A. Wirth ,  Kevin B. Alton ,  James E. Patrick ,  Craig D. Boyle ,  Andrew Stamford

    发明人： Anima Ghosal ,  Wei Tong ,  Swapan K. Chowdhury ,  Shmuel Zbaida ,  Mark A. Wirth ,  Kevin B. Alton ,  James E. Patrick ,  Craig D. Boyle ,  Andrew Stamford

    IPC分类号： C07D473/06 ,  A61K31/522 ,  A61P9/10 ,  A61P9/12

    CPC分类号： C07D473/06

    摘要： The present invention is directed to a metabolite of a xanthine Phosphodiesterase type 5 inhibitor having the following structure derivatives, and formulations thereof, and processes for preparing the same. Further disclosed are methods of treating a physiological disorder, symptom or disease in a patient, comprising administering to the patient an effective amount of the above compound, wherein the physiological disorder, symptom or disease is a urogenital, cardiovascular, cerebrovascular or peripheral vascular disorder, angina pectoris, hypertension, restenosis post angioplasty, endarterectomy, stent introduction, cerebral stroke, a respiratory tract disorder such as an allergic condition associated with atopy, pulmonary hypertension, an ischemic heart disorder, impaired glucose tolerance, diabetes and its related complication, insulin resistance syndrome, hyperglycemia, polycystic ovarian syndrome, a glomerular disorder, renal insufficiency, nephritis, a tubular interstitial disorder, an autoimmune disorder, glaucoma, intestinal motility, cachexia or cancer.

    摘要翻译： 本发明涉及具有以下结构衍生物的黄嘌呤磷酸二酯酶5型抑制剂的代谢物及其制剂及其制备方法。 进一步公开的是治疗患者的生理障碍，症状或疾病的方法，包括向患者施用有效量的上述化合物，其中所述生理障碍，症状或疾病是泌尿生殖系统，心血管，脑血管或外周血管疾病， 心绞痛，高血压，血管成形术后再狭窄，内膜切除术，支架引入，脑中风，呼吸道疾病如与过敏相关的过敏性疾病，肺动脉高压，缺血性心脏病，糖耐量异常，糖尿病及其相关并发症，胰岛素抵抗 综合征，高血糖症，多囊卵巢综合征，肾小球疾病，肾功能不全，肾炎，管状间质性疾病，自身免疫性疾病，青光眼，肠蠕动，恶病质或癌症。

    Piperazine derivatives useful as CCR5 antagonists
    4.
    发明授权
    Piperazine derivatives useful as CCR5 antagonists 有权
    哌嗪衍生物可用作CCR5拮抗剂

    公开(公告)号：US07825121B2

    公开(公告)日：2010-11-02

    申请号：US11255643

    申请日：2005-10-21

    申请人： Ragulan Ramanathan ,  Anima Ghosal ,  Michael W. Miller ,  Swapan K. Chowdhury ,  Kevin B. Alton

    发明人： Ragulan Ramanathan ,  Anima Ghosal ,  Michael W. Miller ,  Swapan K. Chowdhury ,  Kevin B. Alton

    IPC分类号： A61K31/497 ,  A01N43/54 ,  C07D403/00 ,  C07D239/00

    CPC分类号： C07D401/14 ,  C07D401/06 ,  C07H17/02

    摘要： The use of CCR5 antagonists of the formula or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl; R1 is hydrogen or alkyl; R2 is substituted phenyl, substituted heteroaryl, naphthyl, fluorenyl, diphenylmethyl or optionally substituted phenyl- or heteroaryl-alkyl; R3 is hydrogen, alkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, or optionally substituted phenyl, phenylalkyl, naphthyl, naphthylalkyl, heteroaryl or heteroarylalkyl; R4, R5 and R7 are hydrogen or alkyl; R6 is hydrogen, alkyl or alkenyl; for the treatment of HIV, solid organ transplant rejection, graft v. host disease, arthritis, rheumatoid arthritis, inflammatory bowel disease, atopic dermatitis, psoriasis, asthma, allergies or multiple sclerosis is disclosed, as well as novel compounds, pharmaceutical compositions comprising them, and the combination of CCR5 antagonists of the invention in combination with antiviral agents useful in the treatment of HIV or agents useful in the treatment of inflammatory diseases.

    摘要翻译： 使用下式的CCR5拮抗剂或其药学上可接受的盐，其中R是任选取代的苯基，吡啶基，噻吩基或萘基; R1是氢或烷基; R 2是取代的苯基，取代的杂芳基，萘基，芴基，二苯基甲基或任选取代的苯基或杂芳基 - 烷基; R 3是氢，烷基，烷氧基烷基，环烷基，环烷基烷基或任选取代的苯基，苯基烷基，萘基，萘基烷基，杂芳基或杂芳基烷基; R4，R5和R7是氢或烷基; R6是氢，烷基或烯基; 公开了用于治疗HIV，实体器官移植排斥，移植物抗宿主病，关节炎，类风湿性关节炎，炎症性肠病，特应性皮炎，牛皮癣，哮喘，过敏或多发性硬化的新型化合物，以及包含它们的药物组合物 ，以及本发明的CCR5拮抗剂与可用于治疗HIV的抗病毒剂或可用于治疗炎性疾病的药剂的组合。

    Metabolite of xanthine phosphodiesterase 5 inhibitor and derivatives thereof useful for treatment of erectile dysfunction
    5.
    发明申请
    Metabolite of xanthine phosphodiesterase 5 inhibitor and derivatives thereof useful for treatment of erectile dysfunction 失效
    用于治疗勃起功能障碍的黄嘌呤磷酸二酯酶5抑制剂及其衍生物的代谢物

    公开(公告)号：US20050026939A1

    公开(公告)日：2005-02-03

    申请号：US10901574

    申请日：2004-07-29

    申请人： Anima Ghosal ,  Wei Tong ,  Swapan Chowdhury ,  Shmuel Zbaida ,  Mark Wirth ,  Kevin Alton ,  James Patrick ,  Craig Boyle ,  Andrew Stamford

    发明人： Anima Ghosal ,  Wei Tong ,  Swapan Chowdhury ,  Shmuel Zbaida ,  Mark Wirth ,  Kevin Alton ,  James Patrick ,  Craig Boyle ,  Andrew Stamford

    IPC分类号： C07D473/06 ,  A61K31/522 ,  C07D473/02

    CPC分类号： C07D473/06

    摘要： The present invention is directed to a metabolite of a xanthine Phosphodiesterase type 5 inhibitor having the following structure derivatives, and formulations thereof, and processes for preparing the same. Further disclosed are methods of treating a physiological disorder, symptom or disease in a patient, comprising administering to the patient an effective amount of the above compound, wherein the physiological disorder, symptom or disease is a urogenital, cardiovascular, cerebrovascular or peripheral vascular disorder, angina pectoris, hypertension, restenosis post angioplasty, endarterectomy, stent introduction, cerebral stroke, a respiratory tract disorder such as an allergic condition associated with atopy, pulmonary hypertension, an ischemic heart disorder, impaired glucose tolerance, diabetes and its related complication, insulin resistance syndrome, hyperglycemia, polycystic ovarian syndrome, a glomerular disorder, renal insufficiency, nephritis, a tubular interstitial disorder, an autoimmune disorder, glaucoma, intestinal motility, cachexia or cancer.

    摘要翻译： 本发明涉及具有以下结构衍生物的黄嘌呤磷酸二酯酶5型抑制剂的代谢物及其制剂及其制备方法。 进一步公开的是治疗患者的生理障碍，症状或疾病的方法，包括向患者施用有效量的上述化合物，其中所述生理障碍，症状或疾病是泌尿生殖系统，心血管，脑血管或外周血管疾病， 心绞痛，高血压，血管成形术后再狭窄，内膜切除术，支架引入，脑中风，呼吸道疾病如与过敏相关的过敏性疾病，肺动脉高压，缺血性心脏病，糖耐量异常，糖尿病及其相关并发症，胰岛素抵抗 综合征，高血糖症，多囊卵巢综合征，肾小球疾病，肾功能不全，肾炎，管状间质性疾病，自身免疫性疾病，青光眼，肠蠕动，恶病质或癌症。

    Piperazine derivatives useful as CCR5 antagonists
    8.
    发明申请
    Piperazine derivatives useful as CCR5 antagonists 有权
    哌嗪衍生物可用作CCR5拮抗剂

    公开(公告)号：US20060105964A1

    公开(公告)日：2006-05-18

    申请号：US11255643

    申请日：2005-10-21

    申请人： Ragulan Ramanathan ,  Anima Ghosal ,  Michael Miller ,  Swapan Chowdhury ,  Kevin Alton

    发明人： Ragulan Ramanathan ,  Anima Ghosal ,  Michael Miller ,  Swapan Chowdhury ,  Kevin Alton

    IPC分类号： A61K31/7052 ,  A61K31/513 ,  A61K31/506 ,  C07D403/14

    CPC分类号： C07D401/14 ,  C07D401/06 ,  C07H17/02

    摘要： The use of CCR5 antagonists of the formula or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl; R1 is hydrogen or alkyl; R2 is substituted phenyl, substituted heteroaryl, naphthyl, fluorenyl, diphenylmethyl or optionally substituted phenyl- or heteroaryl-alkyl; R3 is hydrogen, alkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, or optionally substituted phenyl, phenylalkyl, naphthyl, naphthylalkyl, heteroaryl or heteroarylalkyl; R4, R5 and R7 are hydrogen or alkyl; R6 is hydrogen, alkyl or alkenyl; for the treatment of HIV, solid organ transplant rejection, graft v. host disease, arthritis, rheumatoid arthritis, inflammatory bowel disease, atopic dermatitis, psoriasis, asthma, allergies or multiple sclerosis is disclosed, as well as novel compounds, pharmaceutical compositions comprising them, and the combination of CCR5 antagonists of the invention in combination with antiviral agents useful in the treatment of HIV or agents useful in the treatment of inflammatory diseases.

    摘要翻译： 使用下式的CCR5拮抗剂或其药学上可接受的盐，其中R是任选取代的苯基，吡啶基，噻吩基或萘基; R 1是氢或烷基; R 2是取代的苯基，取代的杂芳基，萘基，芴基，二苯基甲基或任选取代的苯基或杂芳基 - 烷基; R 3是氢，烷基，烷氧基烷基，环烷基，环烷基烷基或任选取代的苯基，苯基烷基，萘基，萘基烷基，杂芳基或杂芳基烷基; R 4，R 5和R 7是氢或烷基; R 6是氢，烷基或链烯基; 公开了用于治疗HIV，实体器官移植排斥，移植物抗宿主病，关节炎，类风湿性关节炎，炎症性肠病，特应性皮炎，牛皮癣，哮喘，过敏或多发性硬化的新型化合物，以及包含它们的药物组合物 ，以及本发明的CCR5拮抗剂与可用于治疗HIV的抗病毒剂或可用于治疗炎性疾病的药剂的组合。