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1. 发明授权

US09302967B2 Substituted cathechols as inhibitors of IL-4 and IL-5 for the treatment of bronchial asthma 有权
标题翻译：取代的导管胆固醇作为IL-4和IL-5的抑制剂用于治疗支气管哮喘
公开(公告)号：US09302967B2
公开(公告)日：2016-04-05
申请号：US14110869
申请日：2012-04-11
申请人： Santu Bandyopadhyay , Balaram Ghosh , Parasuraman Jaisankar , Bikas Chandra Pal , Siddhartha Roy , Bholanath Paul , Arjun Ram , Ulaganathan Mabalirajan , Nahid Ali , Arun Bandopadhyay , Aditya Konar , Jayashree Bagchi Chakraborty , Indrani Choudhury Mukherjee , Jaydeep Chaudhuri , Sanjit Kumar Mahato , Anirban Manna , Roma Sinha , Pradyot Bhattacharya , Jayaraman Vinayagam , Deba Prasad Jana , Sushovan Chowdhury
发明人： Santu Bandyopadhyay , Balaram Ghosh , Parasuraman Jaisankar , Bikas Chandra Pal , Siddhartha Roy , Bholanath Paul , Arjun Ram , Ulaganathan Mabalirajan , Nahid Ali , Arun Bandopadhyay , Aditya Konar , Jayashree Bagchi Chakraborty , Indrani Choudhury Mukherjee , Jaydeep Chaudhuri , Sanjit Kumar Mahato , Anirban Manna , Roma Sinha , Pradyot Bhattacharya , Jayaraman Vinayagam , Deba Prasad Jana , Sushovan Chowdhury
IPC分类号： A61K31/14 , A61K31/05 , C07C39/19 , A61K31/15 , A61K31/215 , A61K31/277 , A61K31/36 , C07C69/017 , C07C69/732 , C07C251/40 , C07C251/66 , C07C255/36 , C07D317/50
CPC分类号： C07C39/19 , A61K31/05 , A61K31/15 , A61K31/215 , A61K31/277 , A61K31/36 , C07C69/017 , C07C69/732 , C07C251/40 , C07C251/66 , C07C255/36 , C07D317/50
摘要： The present invention relates to compounds of general formula 1 for the treatment of bronchial asthma by inhibition of IL-4 or IL-5 pathway inhibition. The present invention also relates to the use of compound of general formula 1 for the treatment of bronchial by inhibition of IL-4 or IL-5 pathway. The present invention also relates to the method of treating asthma by inhibition of IL-4 or IL-5 pathway by administration of compound or said composition through oral, intranasal, route or by inhalation to a mammal in need thereof. Compound of general formula 1 may be used for reducing perivascular and peribronchial inflammation.
摘要翻译：本发明涉及通过抑制IL-4或IL-5途径抑制来治疗支气管哮喘的通式1的化合物。本发明还涉及通式1化合物通过抑制IL-4或IL-5途径治疗支气管的用途。本发明还涉及通过口服，鼻内，途径或通过吸入需要的哺乳动物施用化合物或所述组合物来抑制IL-4或IL-5途径来治疗哮喘的方法。通式1的化合物可用于减少血管周围和支气管炎。

2. 发明申请

US20140135393A1 SUBSTITUTED CATHECHOLS AS INHIBITORS OF IL-4 AND IL-5 FOR THE TREATMENT BRONCHIAL ASTHMA 审中-公开
标题翻译：作为IL-4和IL-5的抑制剂作为治疗性胆碱性哮喘的替代物
公开(公告)号：US20140135393A1
公开(公告)日：2014-05-15
申请号：US14110869
申请日：2012-04-11
申请人： Santu Bandyopadhyay , Balaram Ghosh , Parasuraman Jaisankar , Bikas Chandra Pal , Siddhartha Roy , Balaram Ghosh , Parasuraman Jaisankar , Bikas Pal , Nahid Ali , Siddhartha Roy , Bholanath Paul , Arjun Ram , Siddhartha Roy , Bholanath Paul , Arjun Ram , Ulaganathan Mabalirajan , Nahid Ali , Arun Bandopadhyay , Aditya Konar , Jayashree Bagchi Chakraborty , Indrani Chowdhury Mukherjee , Jaydeep Chaudhuri , Sanjit Kumar Mahato , Anirban Manna , Roma Sinha , Prayot Bhattacharya , Jayaraman Vinayagam , Deba Prasad Jana , Sushovan Chowdhury
发明人： Santu Bandyopadhyay , Balaram Ghosh , Parasuraman Jaisankar , Bikas Chandra Pal , Siddhartha Roy , Balaram Ghosh , Parasuraman Jaisankar , Bikas Pal , Nahid Ali , Siddhartha Roy , Bholanath Paul , Arjun Ram , Siddhartha Roy , Bholanath Paul , Arjun Ram , Ulaganathan Mabalirajan , Nahid Ali , Arun Bandopadhyay , Aditya Konar , Jayashree Bagchi Chakraborty , Indrani Chowdhury Mukherjee , Jaydeep Chaudhuri , Sanjit Kumar Mahato , Anirban Manna , Roma Sinha , Prayot Bhattacharya , Jayaraman Vinayagam , Deba Prasad Jana , Sushovan Chowdhury
IPC分类号： C07C39/19 , C07C251/40 , C07D317/50 , C07C255/36 , C07C69/732 , C07C69/017 , C07C251/66
CPC分类号： C07C39/19 , A61K31/05 , A61K31/15 , A61K31/215 , A61K31/277 , A61K31/36 , C07C69/017 , C07C69/732 , C07C251/40 , C07C251/66 , C07C255/36 , C07D317/50
摘要： The present invention relates to compounds of general formula 1 for the treatment of bronchial asthma by inhibition of IL-4 or IL-5 pathway inhibition. The present invention also relates to the use of compound of general formula 1 for the treatment of bronchial by inhibition of IL-4 or IL-5 pathway. The present invention also relates to the method of treating asthma by inhibition of IL-4 or IL-5 pathway by administration of compound or said composition through oral, intranasal, route or by inhalation to a mammal in need thereof. Compound of general formula 1 may be used for reducing perivascular and peribronchial inflammation.
摘要翻译：本发明涉及通过抑制IL-4或IL-5途径抑制来治疗支气管哮喘的通式1的化合物。本发明还涉及通式1化合物通过抑制IL-4或IL-5途径治疗支气管的用途。本发明还涉及通过口服，鼻内，途径或通过吸入需要的哺乳动物施用化合物或所述组合物来抑制IL-4或IL-5途径来治疗哮喘的方法。通式1的化合物可用于减少血管周围和支气管炎。

3. 发明申请

US20120283263A1 TRIAZINE-ARYL-BIS-INDOLES AND PROCESS FOR PREPARATION THEREOF 有权
标题翻译：三亚硝基双酚 - 吲哚及其制备方法
公开(公告)号：US20120283263A1
公开(公告)日：2012-11-08
申请号：US13321445
申请日：2010-12-31
申请人： Vasanta Madhava Sharma Gangavaram , Jhillu Singh Yadav , Radha Krishna Palakodety , Arun Bandyopadhyay , Siddhartha Roy , Santu Bandyopadhyay , Rakesh Kamal Johri , Subhash Chander Sharma , Balaram Ghosh , Mabalirajan Ulaganathan , Sakshi Balwani , Bholanath Paul , Ashok Kumar Saxena
发明人： Vasanta Madhava Sharma Gangavaram , Jhillu Singh Yadav , Radha Krishna Palakodety , Arun Bandyopadhyay , Siddhartha Roy , Santu Bandyopadhyay , Rakesh Kamal Johri , Subhash Chander Sharma , Balaram Ghosh , Mabalirajan Ulaganathan , Sakshi Balwani , Bholanath Paul , Ashok Kumar Saxena
IPC分类号： A61K31/53 , A61P11/06 , C12Q1/18 , C07D403/14
CPC分类号： C07D403/14 , A61K31/53 , C07D251/50 , C07D251/52
摘要： A novel heterocyclic compound belonging to ‘triazine-aryl-bis-indoles’, useful for the treatment of asthma. The pathway by which this compound inhibits asthma is also demonstrated. The present invention also provides a process for the preparation of above compounds and their derivatives are presented.
摘要翻译：属于三嗪 - 芳基 - 双 - 吲哚的新型杂环化合物，可用于治疗哮喘。还证明了该化合物抑制哮喘的途径。本发明还提供了制备上述化合物的方法及其衍生物。

4. 发明授权

US09085559B2 Triazine-aryl-bis-indoles and process for preparation thereof 有权
标题翻译：三嗪 - 芳基 - 双 - 吲哚及其制备方法
公开(公告)号：US09085559B2
公开(公告)日：2015-07-21
申请号：US13321445
申请日：2010-12-31
申请人： Vasanta Madhava Sharma Gangavaram , Jhillu Singh Yadav , Radha Krishna Palakodety , Arun Bandyopadhyay , Siddhartha Roy , Santu Bandyopadhyay , Rakesh Kamal Johri , Subhash Chander Sharma , Balaram Ghosh , Mabalirajan Ulaganathan , Sakshi Balwani , Bholanath Paul , Ashok Kumar Saxena
发明人： Vasanta Madhava Sharma Gangavaram , Jhillu Singh Yadav , Radha Krishna Palakodety , Arun Bandyopadhyay , Siddhartha Roy , Santu Bandyopadhyay , Rakesh Kamal Johri , Subhash Chander Sharma , Balaram Ghosh , Mabalirajan Ulaganathan , Sakshi Balwani , Bholanath Paul , Ashok Kumar Saxena
IPC分类号： C07D403/14 , C07D251/50 , C07D251/52 , A61K31/53 , A61P11/06
CPC分类号： C07D403/14 , A61K31/53 , C07D251/50 , C07D251/52
摘要： A novel heterocyclic compound belonging to ‘triazine-aryl-bis-indoles’, useful for the treatment of asthma. The pathway by which this compound inhibits asthma is also demonstrated. The present invention also provides a process for the preparation of above compounds and their derivatives are presented.
摘要翻译：属于“三嗪 - 芳基 - 双 - 吲哚”的新型杂环化合物，可用于治疗哮喘。还证明了该化合物抑制哮喘的途径。本发明还提供了制备上述化合物的方法及其衍生物。

5. 发明申请

US20130131350A1 PYRIDIN-2YL SULFANYL ACID ESTERS AND PROCESS FOR THE PREPARATION THEREOF 失效
标题翻译：吡啶-2YL硫酸酯及其制备方法
公开(公告)号：US20130131350A1
公开(公告)日：2013-05-23
申请号：US13811090
申请日：2011-07-20
申请人： Jadab Chandra Sarma , Dilip Chandra Bora , Paruchuri Gangadhar Rao , Balaram Ghosh , Sakshi Balwani
发明人： Jadab Chandra Sarma , Dilip Chandra Bora , Paruchuri Gangadhar Rao , Balaram Ghosh , Sakshi Balwani
IPC分类号： C07D213/70
CPC分类号： C07D213/70
摘要： The present invention relates to Pyridin-2-yl sulfanyl acid ester compounds having antiinflammatory properties. The present invention particularly relates to novel anti-inflammatory heterocyclic acid esters of Pyridin-2-yl sulfanyl having the structure of general formula 1 which have been screened for their antiinflammatory activity with respect to inhibition of adhesion of neutrophils, isolated from human peripheral blood, onto the surface of human umbilical vein endothelial cells (HU-VEC) as a result of inhibition of the cytokine-stimulated expression of cell adhesion molecule ICAM-1. The compound RS—Z, 3-(Pyridin-2-yl sulfanyl)-propionic acid pentyl ester (structure 1a, R1=H, R2=H, R3=CH2-COOC5H11) was found to be most effective for ICAM-1 and neutrophil adhesion inhibition and was found to effectively alleviate inflammation mediated by excessive leukocyte infiltration leading to inflammatory disorders or like conditions, such as acute lung injury and acute respiratory distress syndrome in mice.
摘要翻译：本发明涉及具有抗炎性质的吡啶-2-基硫基酸酯化合物。本发明特别涉及具有通式1结构的吡啶-2-基硫烷基的新型抗炎杂环酸酯，它们已被筛选出其抗人活性的抑制作用，其中抑制嗜中性粒细胞分离自人外周血，作为抑制细胞因子刺激的细胞粘附分子ICAM-1表达的结果，在人脐静脉内皮细胞（HU-VEC）的表面上。发现化合物RS-Z，3-（吡啶-2-基硫烷基） - 丙酸戊酯（结构1a，R1 = H，R2 = H，R3 = CH2-COOC5H11）对ICAM-1和发现嗜中性粒细胞粘附抑制被发现有效缓解由过度白细胞浸润引起的炎症，导致炎症性疾病或类似病症，如小鼠急性肺损伤和急性呼吸窘迫综合征。

6. 发明授权

US07858763B2 Transforming growth factor beta 1 (TGFβ1) haplotypes and prediction of susceptibility for immunological disorders 失效
标题翻译：转化生长因子β1（TGF＆bgr; 1）单倍型和预测免疫性疾病的易感性
公开(公告)号：US07858763B2
公开(公告)日：2010-12-28
申请号：US11146381
申请日：2005-06-06
申请人： Balaram Ghosh , Shilpy Sharma , Kamalpreet Nagpal
发明人： Balaram Ghosh , Shilpy Sharma , Kamalpreet Nagpal
IPC分类号： C07H21/02 , C07H21/04 , C12Q1/68
CPC分类号： C12Q1/6883 , C12Q2600/106 , C12Q2600/156 , C12Q2600/172
摘要： The present invention is related to the haplotypes of human Transforming Growth Factor Beta1 (TGFβ1) and prediction of susceptibility for immunological disorders. More particularly the present study is the first study in any population, identifying novel protective and risk haplotypes of the TGFβ1 gene The present invention also relates to allelic variants of the human Transforming Growth Factor Beta1 (TGFβ1) gene. The said invention also provides primers and methods suitable for the detection of these haplotypes and allelic variants for the prediction of an individual's disease susceptibility, and/or the genetic analysis of the TGFβ1 gene for immunological disorders, particularly asthma. A vital aspect of the present study provides a method for predicting susceptibility of individuals to immunological disorders, particularly asthma.
摘要翻译：本发明涉及人转化生长因子β1（TGF＆bgr1）的单元型和免疫学障碍易感性的预测。更具体地，本研究是任何人群中首次研究，鉴定TGF-β1基因的新型保护性和风险单倍型本发明还涉及人转化生长因子β1（TGFβB1）基因的等位基因变体。所述发明还提供适于检测这些单倍型和等位基因变体以用于预测个体的疾病易感性的引物和方法，和/或用于免疫学疾病，特别是哮喘的TGFβb基因的遗传分析。本研究的一个重要方面提供了一种预测个体对免疫学疾病，特别是哮喘的易感性的方法。

7. 发明申请

US20060024706A1 Transforming growth factor beta 1 (TGFbeta1) haplotypes and prediction of susceptibility for immunological disorders 失效
标题翻译：转化生长因子β1（TGFbeta1）单倍型和预测免疫性疾病的易感性
公开(公告)号：US20060024706A1
公开(公告)日：2006-02-02
申请号：US11146381
申请日：2005-06-06
申请人： Balaram Ghosh , Shilpy Sharma , Kamalpreet Nagpal
发明人： Balaram Ghosh , Shilpy Sharma , Kamalpreet Nagpal
IPC分类号： C12Q1/68 , C07H21/04 , C12P19/34 , C07K14/495
CPC分类号： C12Q1/6883 , C12Q2600/106 , C12Q2600/156 , C12Q2600/172
摘要： The present invention is related to the haplotypes of human Transforming Growth Factor Beta1 (TGFβ1) and prediction of susceptibility for immunological disorders. More particularly the present study is the first study in any population, identifying novel protective and risk haplotypes of the TGFβ1 gene The present invention also relates to allelic variants of the human Transforming Growth Factor Beta1 (TGFβ1) gene. The said invention also provides primers and methods suitable for the detection of these haplotypes and allelic variants for the prediction of an individual's disease susceptibility, and /or the genetic analysis of the TGFβ1 gene for immunological disorders, particularly asthma. A vital aspect of the present study provides a method for predicting susceptibility of individuals to immunological disorders, particularly asthma.
摘要翻译：本发明涉及人转化生长因子β1（TGFβ1）的单元型和免疫学障碍易感性的预测。更具体地，本研究是任何群体中首次研究，鉴定TGFbeta1基因的新型保护性和风险单倍型本发明还涉及人转化生长因子β1（TGFbeta1）基因的等位基因变体。所述发明还提供适于检测这些单倍型和等位基因变体以用于预测个体的疾病易感性的引物和方法，和/或用于免疫学疾病，特别是哮喘的TGFbeta1基因的遗传分析。本研究的一个重要方面提供了一种预测个体对免疫学疾病，特别是哮喘的易感性的方法。

8. 发明授权

US08680288B2 Pyridin-2yl sulfanyl acid esters and process for the preparation thereof 失效
标题翻译：吡啶-2-基硫基酸酯及其制备方法
公开(公告)号：US08680288B2
公开(公告)日：2014-03-25
申请号：US13811090
申请日：2011-07-20
申请人： Jadab Chandra Sarma , Dilip Chandra Bora , Paruchuri Gangadhar Rao , Balaram Ghosh , Sakshi Balwani
发明人： Jadab Chandra Sarma , Dilip Chandra Bora , Paruchuri Gangadhar Rao , Balaram Ghosh , Sakshi Balwani
IPC分类号： C07D213/62 , A61K31/435
CPC分类号： C07D213/70
摘要： The present invention relates to Pyridin-2-yl sulfanyl acid ester compounds having antiinflammatory properties. The present invention particularly relates to novel anti-inflammatory heterocyclic acid esters of Pyridin-2-yl sulfanyl having the structure of general formula 1 which have been screened for their antiinflammatory activity with respect to inhibition of adhesion of neutrophils, isolated from human peripheral blood, onto the surface of human umbilical vein endothelial cells (HU-VEC) as a result of inhibition of the cytokine-stimulated expression of cell adhesion molecule ICAM-1. The compound RS—Z, 3-(Pyridin-2-yl sulfanyl)-propionic acid pentyl ester (structure 1a, R1=H, R2=H, R3=CH2-COOC5H11) was found to be most effective for ICAM-1 and neutrophil adhesion inhibition and was found to effectively alleviate inflammation mediated by excessive leukocyte infiltration leading to inflammatory disorders or like conditions, such as acute lung injury and acute respiratory distress syndrome in mice.
摘要翻译：本发明涉及具有抗炎性质的吡啶-2-基硫基酸酯化合物。本发明特别涉及具有通式1结构的吡啶-2-基硫烷基的新型抗炎杂环酸酯，它们已被筛选出其抗人活性的抑制作用，其中抑制嗜中性粒细胞分离自人外周血，作为抑制细胞因子刺激的细胞粘附分子ICAM-1表达的结果，在人脐静脉内皮细胞（HU-VEC）的表面上。发现化合物RS-Z，3-（吡啶-2-基硫烷基） - 丙酸戊酯（结构1a，R1 = H，R2 = H，R3 = CH2-COOC5H11）对ICAM-1和发现嗜中性粒细胞粘附抑制被发现有效缓解由过度白细胞浸润引起的炎症，导致炎症性疾病或类似病症，如小鼠急性肺损伤和急性呼吸窘迫综合征。

9. 发明申请

US20070243539A1 GENETIC VARIANTS OF HUMAN INOSITOL POLYPHOSPHATE-4-PHOSPHATASE, TYPE I (INPP4A) USEFUL FOR PREDICTION AND THERAPY OF IMMUNOLOGICAL DISORDER 审中-公开
标题翻译：用于预防和治疗免疫缺陷病毒的人类核苷酸多磷酸酯-4-磷酸酯酶I型（INPP4A）的遗传变异
公开(公告)号：US20070243539A1
公开(公告)日：2007-10-18
申请号：US11552769
申请日：2006-10-25
申请人： Balaram Ghosh , Mamta Sharma , Jyotsna Batra
发明人： Balaram Ghosh , Mamta Sharma , Jyotsna Batra
IPC分类号： C12Q1/68 , C07H21/02 , G01N33/00 , C07H21/04
CPC分类号： C12N9/16 , C12Q1/6883 , C12Q2600/156 , C12Q2600/158 , C12Q2600/172 , Y10T436/143333
摘要： Atopic asthma is a chronic, inflammatory lung disease characterized by recurrent breathing problems in response to an allergen. Platelets play an important role in this allergic inflammatory process, by releasing preformed mediators like platelet factor 4 (PF4) and regulated upon activation in normal T cells expressed and secreted (RANTES) upon activation causing eosinophil chemotaxis. The present invention relates to allelic variants of the human Inositol polyphosphate 4-phosphatase (INPP4A) gene and splice variants of the coding sequence, which encodes INPP4A enzyme known to be an important regulator of platelet activation; and provides primers and methods suitable for the detection of these allelic variants for applications such as molecular diagnosis, prediction and prevention of an individual's disease susceptibility, and/or the genetic analysis of the INPP4A gene in a population. The invention also provides an association with the expression profile of INPP4A protein in the mouse model of asthma. Specifically, the invention provides a method for detection of predisposition to atopic disorders/other immunological disorders such as, autoimmune disorders, inflammatory disorders, cancer, multiple sclerosis, fibrosis, tuberculosis, sarcoidosis, hypertension and disorders developing due to hypertension, diabetes and disorders developing due to diabetes, alcohol abuse, anxiety, asthma, chronic obstructive pulmonary disease (COPD), cholecystectomy, degenerative joint disease (DJD), seizure disorder, arthritis, etc. where human Inositol polyphosphate 4-phosphatase (INPP4A) might play an important role due to its involvement in platelet action.
摘要翻译：特应性哮喘是一种慢性炎性肺病，其特征在于响应于过敏原的复发性呼吸问题。血小板在这种过敏性炎症过程中发挥重要作用，通过释放预先形成的介体如血小板因子4（PF4），并在激活引起嗜酸性粒细胞趋化性的正常T细胞表达和分泌（RANTES）后进行调节。本发明涉及人类肌醇多磷酸酯4-磷酸酶（INPP4A）基因的等位变体和编码序列的剪接变体，其编码已知是血小板活化的重要调节剂的INPP4A酶; 并提供适用于检测这些等位基因变体的引物和方法，用于诸如分子诊断，预测和预防个体疾病易感性的应用，和/或群体中INPP4A基因的遗传分析。本发明还提供了在小鼠哮喘模型中INPP4A蛋白的表达谱的关联。具体地说，本发明提供了一种用于检测特应性疾病/其他免疫性疾病如自身免疫性疾病，炎性疾病，癌症，多发性硬化，纤维化，结核病，结节病，高血压和由高血压发展的病症，糖尿病和发展中的障碍的易感性的方法由于糖尿病，酒精滥用，焦虑症，哮喘，慢性阻塞性肺疾病（COPD），胆囊切除术，退行性关节病（DJD），癫痫发作障碍，关节炎等，其中人类多酚磷酸4-磷酸酶（INPP4A）可能起重要作用由于其参与血小板作用。

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