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1. 发明申请

US20060030588A1 Heteroaryl urea neuropeptide Y Y5 receptor antagonists 有权
公开(公告)号：US20060030588A1
公开(公告)日：2006-02-09
申请号：US11210291
申请日：2005-08-24
申请人： Andrew Stamford , Youhao Dong , Stuart McCombie , Yusheng Wu
发明人： Andrew Stamford , Youhao Dong , Stuart McCombie , Yusheng Wu
IPC分类号： A61K31/4545 , C07D41/14
CPC分类号： C07D401/12 , C07D213/75 , C07D401/14 , C07D403/12 , C07D409/12 , C07D409/14 , C07D417/04 , C07D417/12 , C07D417/14
摘要： The present invention relates to compounds represented by the structural Formula I: or a pharmaceutically acceptable salt thereof, which are useful for the treatment of metabolic and eating disorders such as obesity and hyperphagia, and for the treatment of diabetes and associated disorders.

2. 发明申请

US20050038100A1 Substituted urea neuropeptide Y Y5 receptor antagonists 审中-公开
标题翻译：取代的尿素神经肽Y Y5受体拮抗剂
公开(公告)号：US20050038100A1
公开(公告)日：2005-02-17
申请号：US10933016
申请日：2004-09-01
申请人： William Greenlee , Ying Huang , Joseph Kelly , Stuart McCombie , Andrew Stamford , Yusheng Wu
发明人： William Greenlee , Ying Huang , Joseph Kelly , Stuart McCombie , Andrew Stamford , Yusheng Wu
IPC分类号： C07C275/30 , C07C311/07 , C07D211/58 , C07D211/96 , C07D401/04 , C07D401/06 , C07D409/12 , C07D409/14 , C07D417/04 , A61K31/40 , A61K31/17 , C07D207/46
CPC分类号： C07D401/04 , C07C275/30 , C07C311/07 , C07C2601/14 , C07D211/58 , C07D211/96 , C07D401/06 , C07D409/12 , C07D409/14 , C07D417/04
摘要： A novel class of compounds such as antagonists of the neuropeptide Y Y5 receptor, methods of making such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention or amelioration of one or more diseases associated with the neuropeptide Y Y5 receptor are disclosed.
摘要翻译：一类新颖的化合物，例如神经肽Y Y5受体的拮抗剂，制备此类化合物的方法，含有一种或多种这类化合物的药物组合物，制备包含一种或多种此类化合物的药物制剂的方法，以及治疗，预防或改善方法公开了与神经肽Y Y5受体相关的一种或多种疾病。

3. 发明授权

US07705153B2 Bipiperdine derivatives useful as CCR3 antagonists 失效
标题翻译：双哌啶衍生物可用作CCR3拮抗剂
公开(公告)号：US07705153B2
公开(公告)日：2010-04-27
申请号：US11049460
申请日：2005-02-02
申请人： Pauline C. Ting , Jianhua Cao , Youhao Dong , Eric J. Gilbert , Ying Huang , Joseph M. Kelly , Stuart McCombie , Neng-Yang Shih
发明人： Pauline C. Ting , Jianhua Cao , Youhao Dong , Eric J. Gilbert , Ying Huang , Joseph M. Kelly , Stuart McCombie , Neng-Yang Shih
IPC分类号： A61K31/4709 , A61K31/4725 , C07D215/14
CPC分类号： C07D401/14 , C07D211/18 , C07D211/58 , C07D401/04 , C07D471/04
摘要： The use of CCR3 antagonists of the formula I or a pharmaceutically acceptable salt thereof for the treatment of asthma is disclosed, as well as novel compounds of the formula II, pharmaceutical compositions comprising them, and their use in the treatment of asthma, wherein R, Ra, X, Xa, R1, R2, R2a, R14, R14a, R16 and n are as defined in the specification.
摘要翻译：公开了使用式I的CCR3拮抗剂或其药学上可接受的盐治疗哮喘，以及式II的新型化合物，包含它们的药物组合物及其在治疗哮喘中的用途，其中R， Ra，X，Xa，R1，R2，R2a，R14，R14a，R16和n如说明书中所定义。

4. 发明申请

US20050182095A1 Piperdine derivatives useful as CCR3 antagonists 失效
标题翻译：哌啶衍生物可用作CCR3拮抗剂
公开(公告)号：US20050182095A1
公开(公告)日：2005-08-18
申请号：US11049460
申请日：2005-02-02
申请人： Pauline Ting , Jianhua Cao , Youhao Dong , Eric Gilbert , Ying Huang , Joseph Kelly , Stuart McCombie , Neng-Yang Shih
发明人： Pauline Ting , Jianhua Cao , Youhao Dong , Eric Gilbert , Ying Huang , Joseph Kelly , Stuart McCombie , Neng-Yang Shih
IPC分类号： A61K31/444 , A61K31/4545 , A61K31/4709 , C07D211/18 , C07D211/58 , C07D401/04 , C07D401/14 , C07D413/14 , C07D471/04 , C07D41/14
CPC分类号： C07D401/14 , C07D211/18 , C07D211/58 , C07D401/04 , C07D471/04
摘要： The use of CCR3 antagonists of the formula I or a pharmaceutically acceptable salt thereof for the treatment of asthma is disclosed, as well as novel compounds of the formula II, pharmaceutical compositions comprising them, and their use in the treatment of asthma, wherein R, Ra, X, Xa, R1, R2, R2a, R14, R14a, R16 and n are as defined in the specification.
摘要翻译：公开了使用式I的CCR3拮抗剂或其药学上可接受的盐治疗哮喘，以及式II的新型化合物，包含它们的药物组合物及其在治疗哮喘中的用途，其中R， X 1，X 1，X 2，...，R 2，R 2，R 2， >，R 14，R 14a，R 16和n如说明书中所定义。

5. 发明授权

US4212859A 2'-Hydroxy-2'-desamino-4,6-di-O-(aminoglycosyl)-1,3-diaminocyclitols, methods for their manufacture, method for their use as antibacterial agents, and compositions useful therefor 失效
标题翻译： 2'-脱氧-2'-脱氨基-4,6-二-O-（氨基糖基）-1,3-二氨基环糊精，其制备方法，其用作抗菌剂的方法和可用于其的组合物
公开(公告)号：US4212859A
公开(公告)日：1980-07-15
申请号：US912603
申请日：1978-06-05
申请人： Peter J. L. Daniels , Stuart McCombie , Tattanahalli L. Nagabhushan
发明人： Peter J. L. Daniels , Stuart McCombie , Tattanahalli L. Nagabhushan
IPC分类号： C07H15/234 , A61K31/71 , C07H15/22
CPC分类号： C07H15/234 , Y02P20/55
摘要： 2'-Hydroxy-2'-desamino-4,6-di-O-(aminoglycosyl)-1,3-diaminocyclitols having a 6'-amino function exhibit antibacterial activity and are prepared by reaction of the corresponding N-protected (except the 2'-amino)-4,6-di-O-(aminoglycosyl)-1,3-diaminocyclitol with hydrogen peroxide in the presence of tungstate ion, followed by cleavage of the thereby formed 2'-oximino derivative, thence reduction of the resulting 2'-oxo derivative and removal of the N-protecting groups.Preferred compounds are 1-N-(.omega.-amino-.alpha.-hydroxyalkanoyl)-2'-hydroxy-2'-desamino-4,6-di-O-(aminoglycosyl)-1,3-diaminocyclitols which exhibit antibacterial activity against bacteria resistant to the parent aminoglycoside.
摘要翻译：具有6'-氨基功能的2'-羟基-2'-脱氨基-4,6-二-O-（氨基糖基）-1,3-二氨基二醇具有抗菌活性，并通过相应的N-保护（除 2'-氨基）-4,6-二-O-（氨基糖基）-1,3-二氨基环糊精与过氧化氢在钨酸根离子存在下，然后裂解由此形成的2'-肟基衍生物，从而减少得到的2'-氧代衍生物和N-保护基团的除去。优选的化合物是对细菌具有抗菌活性的1-N-（ω-氨基-α-羟基烷酰基）-2'-羟基-2'-脱氨基-4,6-二-O-（氨基糖基）-1,3-二氨基二醇对母体氨基糖苷类具有抗性。

6. 发明申请

US20060223856A1 Piperidinyl piperidine derivatives useful as inhibitors of chemokine receptors 失效
标题翻译：可用作趋化因子受体抑制剂的哌啶基哌啶衍生物
公开(公告)号：US20060223856A1
公开(公告)日：2006-10-05
申请号：US11358248
申请日：2006-02-21
申请人： Tze-Ming Chan , Kathleen Cox , Wenqing Feng , Michael Miller , Daniel Weston , Stuart McCombie
发明人： Tze-Ming Chan , Kathleen Cox , Wenqing Feng , Michael Miller , Daniel Weston , Stuart McCombie
IPC分类号： A61K31/4545 , C07D403/14
CPC分类号： C07D401/14
摘要： In its many embodiments, the present invention provides a novel class of compounds of structural formula IA or IB where R1-R8 are as disclosed herein as inhibitors of the CCR5 receptors, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with CCR5 using such compounds or pharmaceutical compositions. The invention also relates to the use of a combination of a compound of this invention and one or more antiviral or other agents useful in the treatment of Human Immunodeficiency Virus (HIV). The invention further relates to the use of a compound of this invention, alone or in combination with another agent, in the treatment of solid organ transplant rejection, graft v. host disease, arthritis, rheumatoid arthritis, inflammatory bowel disease, atopic dermatitis, psoriasis, asthma, allergies or multiple sclerosis.
摘要翻译：在其许多实施方案中，本发明提供了一类新颖结构式IA或IB的化合物，其中R 1至R 8如本文所公开的CCR5受体的抑制剂制备这些化合物的方法，含有一种或多种这样的化合物的药物组合物，制备包含一种或多种这类化合物的药物制剂的方法，以及使用这种化合物治疗，预防，抑制或改善与CCR5相关的一种或多种疾病的方法或药物组合物。本发明还涉及本发明化合物与一种或多种可用于治疗人类免疫缺陷病毒（HIV）的抗病毒剂或其它药剂的组合的用途。本发明还涉及本发明化合物单独或与另一种药剂组合用于治疗实体器官移植排斥，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。

7. 发明申请

US20060100228A1 Cannabinoid receptor ligands 失效
标题翻译：大麻素受体配体
公开(公告)号：US20060100228A1
公开(公告)日：2006-05-11
申请号：US11157510
申请日：2005-06-21
申请人： Bandarpalle Shankar , Eric Gilbert , Razia Rizvi , Chunli Huang , Joseph Kozlowski , Stuart McCombie , Neng-Yang Shih
发明人： Bandarpalle Shankar , Eric Gilbert , Razia Rizvi , Chunli Huang , Joseph Kozlowski , Stuart McCombie , Neng-Yang Shih
IPC分类号： A61K31/4747 , A61K31/46 , A61K31/405 , C07D455/02 , C07D403/02
CPC分类号： C07D221/20 , C07D209/52 , C07D401/12 , C07D471/08
摘要： Compounds of Formula I: and/or pharmaceutically acceptable salts, solvates or prodrugs thereof, or pharmaceutical compositions containing such compounds exhibit anti-inflammatory and immunomodulatory activity, and can be effective in treating cancer and inflammatory, immunomodulatory or respiratory diseases or conditions.
摘要翻译：式I化合物和/或其药学上可接受的盐，溶剂化物或前药，或含有这些化合物的药物组合物表现出抗炎和免疫调节活性，并且可有效治疗癌症和炎症，免疫调节或呼吸系统疾病或病症。

8. 发明申请

US20060247320A1 Compounds for inhibiting KSP kinesin activity 审中-公开
标题翻译：抑制KSP驱动蛋白活性的化合物
公开(公告)号：US20060247320A1
公开(公告)日：2006-11-02
申请号：US11369643
申请日：2006-03-07
申请人： Jayaram Tagat , Timothy Guzi , Marc Labroli , Cory Poker , Yushi Xiao , Angela Kerekes , Tao Yu , Sunil Paliwal , Hon-Chung Tsui , Neng-Yang Shih , Stuart McCombie , Vincent Madison , Charles Lesburg , Jose Duca
发明人： Jayaram Tagat , Timothy Guzi , Marc Labroli , Cory Poker , Yushi Xiao , Angela Kerekes , Tao Yu , Sunil Paliwal , Hon-Chung Tsui , Neng-Yang Shih , Stuart McCombie , Vincent Madison , Charles Lesburg , Jose Duca
IPC分类号： A61K31/12
CPC分类号： C07D519/00 , C07D493/10 , C07D495/04 , C07D495/06 , C07D495/14 , C07D495/20 , C07D513/04
摘要： The present invention provides compounds of Formula I (wherein R1, R3, X, W, Z and ring Y are as defined herein). The present invention also provides compositions comprising these compounds that are useful for treating cellular proliferative diseases or disorders associated with KSP kinesin activity and for inhibiting KSP kinesin activity.
摘要翻译：本发明提供式I化合物（其中R 1，R 3，X，W，Z和环Y如本文所定义）。本发明还提供了包含这些化合物的组合物，其可用于治疗与KSP驱动蛋白活性相关的细胞增殖性疾病或病症并抑制KSP驱动蛋白活性。

9. 发明授权

US07750158B2 Cannabinoid receptor ligands 失效
标题翻译：大麻素受体配体
公开(公告)号：US07750158B2
公开(公告)日：2010-07-06
申请号：US11157510
申请日：2005-06-21
申请人： Bandarpalle B. Shankar , Eric Gilbert , Razia K. Rizvi , Chunli Huang , Joseph A. Kozlowski , Stuart McCombie , Neng-Yang Shih
发明人： Bandarpalle B. Shankar , Eric Gilbert , Razia K. Rizvi , Chunli Huang , Joseph A. Kozlowski , Stuart McCombie , Neng-Yang Shih
IPC分类号： C07D221/00 , A61K31/44
CPC分类号： C07D221/20 , C07D209/52 , C07D401/12 , C07D471/08
摘要： Compounds of Formula I: and/or pharmaceutically acceptable salts, solvates or prodrugs thereof, or pharmaceutical compositions containing such compounds exhibit anti-inflammatory and immunomodulatory activity, and can be effective in treating cancer and inflammatory, immunomodulatory or respiratory diseases or conditions.
摘要翻译：式I化合物和/或其药学上可接受的盐，溶剂化物或前药，或含有这些化合物的药物组合物表现出抗炎和免疫调节活性，并且可有效治疗癌症和炎症，免疫调节或呼吸系统疾病或病症。

10. 发明申请

US20060223821A1 Piperidinyl piperazine derivatives useful as inhibitors of chemokine receptors 失效
标题翻译：可用作趋化因子受体抑制剂的哌啶基哌嗪衍生物
公开(公告)号：US20060223821A1
公开(公告)日：2006-10-05
申请号：US11358520
申请日：2006-02-21
申请人： Tze-Ming Chan , Kathleen Cox , Wenqing Feng , Michael Miller , Daniel Weston , Stuart McCombie
发明人： Tze-Ming Chan , Kathleen Cox , Wenqing Feng , Michael Miller , Daniel Weston , Stuart McCombie
IPC分类号： A61K31/496 , C07D403/14
CPC分类号： C07D211/96 , C07D401/06 , C07D401/14
摘要： In its many embodiments, the present invention provides a novel class of compounds of structural formula IA or IB where R1-R8 are as disclosed herein as inhibitors of the CCR5 receptors, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with CCR5 using such compounds or pharmaceutical compositions. The invention also relates to the use of a combination of a compound of this invention and one or more antiviral or other agents useful in the treatment of Human Immunodeficiency Virus (HIV). The invention further relates to the use of a compound of this invention, alone or in combination with another agent, in the treatment of solid organ transplant rejection, graft v. host disease, arthritis, rheumatoid arthritis, inflammatory bowel disease, atopic dermatitis, psoriasis, asthma, allergies or multiple sclerosis.
摘要翻译：在其许多实施方案中，本发明提供了一类新颖结构式IA或IB的化合物，其中R 1至R 8如本文所公开的CCR5受体的抑制剂制备这些化合物的方法，含有一种或多种这样的化合物的药物组合物，制备包含一种或多种这类化合物的药物制剂的方法，以及使用这种化合物治疗，预防，抑制或改善与CCR5相关的一种或多种疾病的方法或药物组合物。本发明还涉及本发明化合物与一种或多种可用于治疗人类免疫缺陷病毒（HIV）的抗病毒剂或其它药剂的组合的用途。本发明还涉及本发明化合物单独或与另一种药剂组合用于治疗实体器官移植排斥，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。

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