专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

WO2005094819A1 METHIMAZOLE DERIVATIVES AND TAUTOMERIC CYCLIC THIONES TO INHIBIT CELL ADHESION 审中-公开
标题翻译：甲基咪唑衍生物和紫外线循环阻止细胞粘附
公开(公告)号：WO2005094819A1
公开(公告)日：2005-10-13
申请号：PCT/US2004/007888
申请日：2004-03-16
申请人： INTERTHYR CORPORATION , KOHN, Leonard, D. , GOETZ, Douglas , HARI, Norikazu , LEWIS, Chris , GIULIANI, Cesidio , NAPOLITANO, Giorgio , DAGIA, Nilesh
发明人： KOHN, Leonard, D. , GOETZ, Douglas , HARI, Norikazu , LEWIS, Chris , GIULIANI, Cesidio , NAPOLITANO, Giorgio , DAGIA, Nilesh
IPC分类号： A61K31/415
CPC分类号： A61K31/415 , Y02A50/411
摘要： The present invention relates to novel compounds and methods of use for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. This invention also relates to pharmaceutical formulations comprising these compounds and methods of using them for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. The compounds and pharmaceutical compositions of this invention can be used as therapeutic or prophylactic agents. In particular, methimazole derivatives and tautomeric cyclic thiones have the ability to inhibit the adhesion and the migration of leukocytes. In addition to being active antiinflammatories, the methimazole derivatives and tautomeric cyclic thiones and their physiologically tolerable salts, derivatives and prodrugs are generally suitable for the treatment (i.e., for the therapy and prophylaxis) of diseases that are based on the interaction between VCAM-1 and its ligands or can be influenced by an inhibition of this interaction. In particular, the methimazole derivatives and tautomeric cyclic thiones are suitable for the treatment of diseases that are caused at least partly by an undesired extent of leukocyte adhesion and/or leukocyte migration or are connected therewith, and for whose prevention, alleviation or cure the adhesion and/or migration of leukocytes should be decreased.
摘要翻译：本发明涉及新型化合物和用于抑制和预防细胞粘附和细胞粘附介导的病理学的方法。本发明还涉及包含这些化合物的药物制剂及其用于抑制和预防细胞粘附和细胞粘附介导的病理学的方法。本发明的化合物和药物组合物可用作治疗剂或预防剂。特别地，甲巯咪唑衍生物和互变异构环状硫堇具有抑制白细胞粘附和迁移的能力。除了是有效的抗炎剂之外，甲巯咪唑衍生物和互变异构环状硫堇及其生理上可耐受的盐，衍生物和前药通常适用于基于VCAM-1之间的相互作用的疾病的治疗（即治疗和预防）和它的配体或可能受到这种相互作用的抑制的影响。特别地，甲巯咪唑衍生物和互变异构环状硫堇适用于治疗至少部分由不期望的白细胞粘附和/或白细胞迁移程度引起的疾病或与之相关的疾病，并且为了预防，缓解或治愈粘连和/或白细胞迁移应减少。

2. 发明申请

WO2011055320A1 IMIDAZOPYRIDINE DERIVATIVES 审中-公开
标题翻译：咪唑吡啶衍生物
公开(公告)号：WO2011055320A1
公开(公告)日：2011-05-12
申请号：PCT/IB2010/054996
申请日：2010-11-04
申请人： PIRAMAL LIFE SCIENCES LIMITED , KUMAR, Sanjay , HARIHARAN, Sivaramakrishnan , BHONDE, Mandar , DAGIA, Nilesh , SHARMA, Rajiv , MANE, Pallavi Hanmantrao , KUMAR, Pramod Bhaskar
发明人： KUMAR, Sanjay , HARIHARAN, Sivaramakrishnan , BHONDE, Mandar , DAGIA, Nilesh , SHARMA, Rajiv , MANE, Pallavi Hanmantrao , KUMAR, Pramod Bhaskar
IPC分类号： C07D471/04 , A61K31/437 , A61P35/00
CPC分类号： C07D471/04
摘要： The present invention relates to compounds of formula (I), wherein R a , R b , R c , R d , R e and R f are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases mediated by phosphatidylinositol-3-kinase (PBK), mammalian target of rapamycin (mTOR), Signal transducer and activator of transcription 3 (STAT 3), tumor necrosis factor-α (TNF-α), interleukin-6 (IL-6) or a combination thereof particularly in the treatment of cancer and inflammation.
摘要翻译：本发明涉及式（I）化合物，其中Ra，Rb，Rc，Rd，Re和Rf如本说明书中所定义，其制备方法，含有它们的药物组合物及其在治疗由磷脂酰肌醇-3-激酶（PBK），雷帕霉素哺乳动物靶（mTOR），信号转导和转录激活因子3（STAT3），肿瘤坏死因子-α（TNF-α），白细胞介素-6（IL-6）或特别是在治疗癌症和炎症中的组合。

3. 发明申请

WO2009019656A1 PYRIDYL DERIVATIVES, THEIR PREPARATION AND USE 审中-公开
标题翻译：吡啶衍生物，其制备和使用
公开(公告)号：WO2009019656A1
公开(公告)日：2009-02-12
申请号：PCT/IB2008/053151
申请日：2008-08-06
申请人： PIRAMAL LIFE SCIENCES LIMITED , KUMAR, Sanjay , JOSHI, Kalpana, Sanjay , DEORE, Vijaykumar , BHONDE, Mandar, Ramesh , YEWALKAR, Nilambari, Nilkanth , PADGAONKAR, Amol, Arun , RATHOS, Maggie, Joyce , KULKARNI-ALMEIDA, Asha, Adrian , PARIKH, Sapna , DAGIA, Nilesh, Madhukar
发明人： KUMAR, Sanjay , JOSHI, Kalpana, Sanjay , DEORE, Vijaykumar , BHONDE, Mandar, Ramesh , YEWALKAR, Nilambari, Nilkanth , PADGAONKAR, Amol, Arun , RATHOS, Maggie, Joyce , KULKARNI-ALMEIDA, Asha, Adrian , PARIKH, Sapna , DAGIA, Nilesh, Madhukar
IPC分类号： C07D213/73 , C07D213/75 , C07D213/78 , C07D401/04 , C07D407/04 , C07D413/04 , A61K31/44 , A61K31/4439 , A61K31/00
CPC分类号： C07D213/73 , C07D213/75 , C07D213/78 , C07D401/04 , C07D407/04 , C07D413/04
摘要： The present invention relates to pyridyl derivatives capable of inhibiting phosphatidylinositol-3-kinase (PI3k), mammalian target of rapamycin (mTOR) and/or hypoxia inducible factor 1α (HIF-1α) mediated signaling. Also disclosed are processes for preparation of the pyridyl derivatives, and their use in the manufacture of pharmaceutical compositions for the treatment of clinical conditions caused by deregulation of signaling pathways selected from one or more of PI3K, mTOR and HIF-1α pathways. The pyridyl derivatives are also useful for the treatment of conditions or disorders mediated by TNF-α.
摘要翻译：本发明涉及能够抑制磷脂酰肌醇-3-激酶（PI3k），雷帕霉素哺乳动物靶（mTOR）和/或缺氧诱导因子1a（HIF-1a）介导信号传导的吡啶衍生物。还公开了制备吡啶基衍生物的方法及其在制备用于治疗由选自PI3K，mTOR和HIF-1a途径中的一种或多种的信号传导途径失调引起的临床病症的药物组合物中的用途。吡啶基衍生物也可用于治疗由TNF-α介导的病症或病症。

4. 发明申请

WO2006019962A1 COMPOSITIONS AND METHODS FOR TREATMENT OF COLITIS 审中-公开
标题翻译：用于治疗结肠炎的组合物和方法
公开(公告)号：WO2006019962A1
公开(公告)日：2006-02-23
申请号：PCT/US2005/025067
申请日：2005-07-14
申请人： INTERTHYR CORPORATION , KOHN, Leonard, D. , GOETZ, Douglas, J. , BENAVIDES-PERALTA, Uruguaysito , GONZALEZ-MURGUIONDO, Marianna , HARII, Norikazu , LEWIS, Christopher, J. , NAPOLITANO, Giorgio , DAGIA, Nilesh, D.
发明人： KOHN, Leonard, D. , GOETZ, Douglas, J. , BENAVIDES-PERALTA, Uruguaysito , GONZALEZ-MURGUIONDO, Marianna , HARII, Norikazu , LEWIS, Christopher, J. , NAPOLITANO, Giorgio , DAGIA, Nilesh, D.
IPC分类号： A61K31/4164
CPC分类号： A61K31/4164 , Y02A50/402 , Y02A50/411
摘要： The present invention relates to the treatment of inflammatory bowel disease (IBD) and related gastrointestinal pathologies. This invention also relates to the treatment of cytokine-mediated diseases, including tumor necrosis factor-α (TNFα)-induced diseases and/or chemokine-mediated diseases. This invention also relates to treating an animal having a disease or condition associated with Toll-like receptor (4). Specifically, the present invention relates to the treatment of inflammatory bowel disease (IBD) and related gastrointestinal pathologies that are cytokine-mediated or associated with Toll-like receptor (4). More specifically, this invention is directed to methods for treating or preventing IBD and related gastrointestinal pathologies using methimazole derivatives and tautomeric cyclic thiones. This invention is also directed to pharmaceutical compositions containing methimazole derivatives and tautomeric cyclic thiones, which are useful for the treatment or prophylaxis of IBD and related gastrointestinal pathologies. This invention also relates to pharmaceutical formulations capable of inhibiting tumor necrosis factor-α (TNFα)-induced vascular cell adhesion molecule-1 (VCAM-1) expression and the resulting leukocyte-endothelial cell adhesion for the inhibition and prevention of inflammatory bowel syndrome and related gastrointestinal pathologies.
摘要翻译：本发明涉及治疗炎性肠病（IBD）和相关的胃肠病理。本发明还涉及治疗细胞因子介导的疾病，包括肿瘤坏死因子-α（TNFα）诱导的疾病和/或趋化因子介导的疾病。本发明还涉及治疗具有与Toll样受体（4）相关的疾病或病症的动物。具体而言，本发明涉及炎症性肠病（IBD）和细胞因子介导的或与Toll样受体（4）相关的相关胃肠病理的治疗。更具体地，本发明涉及使用甲巯咪唑衍生物和互变异构环状硫酮治疗或预防IBD和相关胃肠病理的方法。本发明还涉及含有甲巯咪唑衍生物和互变异构环状硫堇的药物组合物，其可用于治疗或预防IBD和相关的胃肠病理。本发明还涉及能够抑制肿瘤坏死因子-α（TNFα） - 诱导的血管细胞粘附分子-1（VCAM-1）表达和由此产生的白细胞 - 内皮细胞粘附的药物制剂，用于抑制和预防炎性肠综合征和相关的胃肠病变。

5. 发明申请

WO2012077031A1 SUBSTITUTED IMIDAZOQUINOLINE DERIVATIVES 审中-公开
标题翻译：取代的咪唑啉醇衍生物
公开(公告)号：WO2012077031A1
公开(公告)日：2012-06-14
申请号：PCT/IB2011/055449
申请日：2011-12-05
申请人： PIRAMAL LIFE SCIENCES LIMITED , KUMAR, Sanjay , SHARMA, Rajiv , DEORE, Vijaykumar Bhagwan , YEWALKAR, Nilambari Nilkanth , AGARWAL, Veena R , DAGIA, Nilesh , NAIK, Nishigandha
发明人： KUMAR, Sanjay , SHARMA, Rajiv , DEORE, Vijaykumar Bhagwan , YEWALKAR, Nilambari Nilkanth , AGARWAL, Veena R , DAGIA, Nilesh , NAIK, Nishigandha
IPC分类号： A61K31/4745 , C07D471/04 , A61P29/00
CPC分类号： C07D471/04
摘要： The present invention relates to substituted imidazo[4,5-c]quinoline derivatives of formula (I), wherein R 1 , R 2 and R 3 are as defined in the specification, processes for their preparation, pharmaceutical compositions comprising compounds of the present invention and their use in the treatment of diseases or disorders mediated by one or more kinases, particularly proliferative diseases or disorders such as cancer. These compounds can also be used in the treatment of inflammation and angiogenesis related disorders.
摘要翻译：本发明涉及式（I）的取代的咪唑并[4,5-c]喹啉衍生物，其中R 1，R 2和R 3如说明书中所定义，其制备方法，包含本发明化合物的药物组合物及其制备方法用于治疗由一种或多种激酶介导的疾病或病症，特别是增殖性疾病或疾病如癌症。这些化合物也可用于治疗炎症和血管发生相关疾病。

6. 发明申请

WO2011061667A1 USE OF MACROCYCLIC LACTONE DERIVATIVES FOR THE TREATMENT OF INFLAMMATORY DISORDERS 审中-公开
标题翻译：用于治疗炎症性疾病的大环激素衍生物的使用
公开(公告)号：WO2011061667A1
公开(公告)日：2011-05-26
申请号：PCT/IB2010/055162
申请日：2010-11-15
申请人： PIRAMAL LIFE SCIENCES LIMITED , KULKARNI-ALMEIDA, Asha , GUPTE, Ravindra Dattatray , DAGIA, Nilesh Madhukar , MISHRA, Prabha Beerchandra
发明人： KULKARNI-ALMEIDA, Asha , GUPTE, Ravindra Dattatray , DAGIA, Nilesh Madhukar , MISHRA, Prabha Beerchandra
IPC分类号： A61K31/365 , A61P43/00 , A61P31/18 , A61P9/10
CPC分类号： A61K31/365 , Y02A50/411
摘要： The present invention provides use of the compounds represented by formula (1): wherein, R 1 , R 2 , R 3 and R 4 are as defined in the specification, in all their stereo isomeric and tautomeric forms and mixtures thereof in all ratios, and their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, pharmaceutically acceptable polymorphs and prodrugs and pharmaceutical compositions containing them for treatment of inflammatory disorders mediated by one or more cytokines selected from Tumor Necrosis Factor-alpha (TNF-α), interferon-γ (IFN-γ) and interleukins such as IL-lβ, IL-2, IL-6, and IL-8. The present invention also relates to a pharmaceutical composition adapted for use in the treatment of inflammatory disorders. The present invention further provides a method of treatment of inflammatory disorders by administering a therapeutically effective amount of the said compound of formula (1) or its pharmaceutical composition, to a mammal in need thereof.
摘要翻译：本发明提供由式（1）表示的化合物的用途：其中R1，R2，R3和R4如说明书中所定义，具有所有比例的所有立体异构体和互变异构形式及其混合物及其药学上可接受的盐，药学上可接受的溶剂合物，药学上可接受的多晶型物和前药以及含有它们的药物组合物，用于治疗由一种或多种选自肿瘤坏死因子-α（TNF-α），干扰素-α （IFN-α）和白细胞介素如IL-1β，IL-2，IL-6和IL-8。本发明还涉及适用于治疗炎症性疾病的药物组合物。本发明还提供了通过向有需要的哺乳动物施用治疗有效量的所述式（1）化合物或其药物组合物来治疗炎症性疾病的方法。

7. 发明申请

WO2006019962B1 COMPOSITIONS AND METHODS FOR TREATMENT OF COLITIS 审中-公开
标题翻译：用于治疗患者的组合物和方法
公开(公告)号：WO2006019962B1
公开(公告)日：2006-04-20
申请号：PCT/US2005025067
申请日：2005-07-14
申请人： INTERTHYR CORP , KOHN LEONARD D , GOETZ DOUGLAS J , BENAVIDES-PERALTA URUGUAYSITO , GONZALEZ-MURGUIONDO MARIANNA , HARII NORIKAZU , LEWIS CHRISTOPHER J , NAPOLITANO GIORGIO , DAGIA NILESH D
发明人： KOHN LEONARD D , GOETZ DOUGLAS J , BENAVIDES-PERALTA URUGUAYSITO , GONZALEZ-MURGUIONDO MARIANNA , HARII NORIKAZU , LEWIS CHRISTOPHER J , NAPOLITANO GIORGIO , DAGIA NILESH D
IPC分类号： A61K31/4164 , A61P1/04
CPC分类号： A61K31/4164
摘要： The present invention relates to the treatment of inflammatory bowel disease (IBD) and related gastrointestinal pathologies. This invention also relates to the treatment of cytokine-mediated diseases, including tumor necrosis factor-a (TNFa)-induced diseases and/or chemokine-mediated diseases. This invention also relates to treating an animal having a disease or condition associated with Toll-like receptor (4). Specifically, the present invention relates to the treatment of inflammatory bowel disease (IBD) and related gastrointestinal pathologies that are cytokine-mediated or associated with Toll-like receptor (4). More specifically, this invention is directed to methods for treating or preventing IBD and related gastrointestinal pathologies using methimazole derivatives and tautomeric cyclic thiones. This invention is also directed to pharmaceutical compositions containing methimazole derivatives and tautomeric cyclic thiones, which are useful for the treatment or prophylaxis of IBD and related gastrointestinal pathologies. This invention also relates to pharmaceutical formulations capable of inhibiting tumor necrosis factor-a (TNFa)-induced vascular cell adhesion molecule-1 (VCAM-1) expression and the resulting leukocyte-endothelial cell adhesion for the inhibition and prevention of inflammatory bowel syndrome and related gastrointestinal pathologies.
摘要翻译：本发明涉及炎症性肠病（IBD）和相关胃肠道病理学的治疗。本发明还涉及细胞因子介导的疾病的治疗，包括肿瘤坏死因子-α（TNFα）诱导的疾病和/或趋化因子介导的疾病。本发明还涉及治疗具有与Toll样受体相关的疾病或病症的动物（4）。具体地，本发明涉及炎性肠病（IBD）和细胞因子介导的或与Toll样受体相关的相关胃肠道病理学的治疗（4）。更具体地，本发明涉及使用甲巯咪唑衍生物和互变异构环状硫堇治疗或预防IBD和相关胃肠道病理学的方法。本发明还涉及含有甲巯咪唑衍生物和互变异构环状硫堇的药物组合物，其可用于治疗或预防IBD和相关的胃肠道病理。本发明还涉及能够抑制肿瘤坏死因子-α（TNFα）诱导的血管细胞粘附分子-1（VCAM-1）表达的药物制剂以及由此产生的白细胞内皮细胞粘附以抑制和预防炎症性肠综合征，相关的胃肠道病变。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式