公开(公告)号：US20090036356A1

公开(公告)日：2009-02-05

申请号：US11714663

申请日：2007-03-06

申请人： Villoo Morawala Patell ,  Akash Mathur ,  Amitesh Suman ,  V. Fredrick Devadoss

发明人： Villoo Morawala Patell ,  Akash Mathur ,  Amitesh Suman ,  V. Fredrick Devadoss

IPC分类号： A61K38/28 ,  C07C57/30 ,  A61K38/17 ,  C40B30/02 ,  A61K31/455 ,  A61K31/195

CPC分类号： C07C53/126 ,  G16B15/00 ,  G16B35/00 ,  G16C20/60

摘要： The present invention is directed to novel Octanoic acid derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DPP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, particularly in the treatment of type 2 diabetes and conditions that are associated with the same. In addition, the present invention provides pharmaceutical compositions useful in inhibiting DPP-IV enzyme, comprising a therapeutically effective amount of Octanoic acid derivatives. Moreover, the present invention provides a method of inhibiting DPP-IV comprising administering to a mammal in need of such treatment a therapeutically effective amount of a single or a combination of Octanoic acid derivatives of the invention.The invention further relates to the kits and other articles of manufacture for treating disease states associated with DPP-IV enzyme.The invention further relates to a method of identifying a compound that has dipeptidyl peptidase-IV enzyme inhibition activity, comprising following steps: 1. Define the residues of the active site of DPP-IV 2. Define the geometry and force field relationship of the residues identified above in (1) 3. Define the physical parameters of the active site identified in (1) 4. Validate the model based on mutational analysis and in-vitro inhibitor binding studies 5. Screen the library for scaffolds and small molecules that satisfy the model developed in (3) and validated in (4) above. 6. Dock each inhibitor identified in (5) above to the active site of DPP-IV defined in (1). 7. Minimize the energy of the inhibitor and DPP-IV complex using force fields used in (2) above. 8. Compare the energy of interaction of each inhibitor to that of known inhibitors. 9. Synthesize and validate in in-vitro assays

摘要翻译： 本发明涉及作为二肽基肽酶-IV酶抑制剂的新型辛酸衍生物（“DPP-IV抑制剂”），其可用于治疗或预防涉及二肽基肽酶-IV酶的疾病， 特别是在治疗2型糖尿病和与之相关的病症方面。 此外，本发明提供了可用于抑制DPP-IV酶的药物组合物，其包含治疗有效量的辛酸衍生物。 此外，本发明提供抑制DPP-IV的方法，包括向需要这种治疗的哺乳动物施用治疗有效量的本发明的辛酸衍生物的单一或组合。 本发明还涉及用于治疗与DPP-IV酶相关的疾病状态的试剂盒和其它制品。 本发明还涉及鉴定具有二肽基肽酶-IV酶抑制活性的化合物的方法，包括以下步骤：1.定义DPP-IV的活性位点的残基2.定义残基的几何形状和力场关系 （1）中确定的活性位点的物理参数定义（1）中确定的活性位点的物理参数4.基于突变分析和体外抑制剂结合研究验证模型5.筛选满足以下条件的支架和小分子的文库 （3）中开发并在上述（4）中验证的模型。 6.将上述（5）中鉴定的每种抑制剂停留在（1）中定义的DPP-IV的活性位点。 7.使用上述（2）中使用的力场，最小化抑制剂和DPP-IV复合物的能量。 8.比较每个抑制剂与已知抑制剂相互作用的能量。 9.在体外测定中合成和验证

公开(公告)号：US20110190482A1

公开(公告)日：2011-08-04

申请号：US12997215

申请日：2009-06-10

申请人： Villoo Morawala Patell ,  Rajesh Ullanat ,  Thippeswamy Sidegonde ,  Sunil Shekar ,  Sunit Maity ,  Chellappa Gopalakrishnan ,  Sami Noshir Guzder

发明人： Villoo Morawala Patell ,  Rajesh Ullanat ,  Thippeswamy Sidegonde ,  Sunil Shekar ,  Sunit Maity ,  Chellappa Gopalakrishnan ,  Sami Noshir Guzder

IPC分类号： C07H21/00 ,  C40B20/00

CPC分类号： C12N15/1089 ,  G16B20/00 ,  G16B25/00

摘要： The present invention relates to use of novel bioinformatics approach for predicting and identifying Scaffold/Matrix attachment regions (S/MARs) from different genomic database.

摘要翻译： 本发明涉及新型生物信息学方法用于从不同基因组数据库预测和鉴定支架/基质附着区域（S / MAR）的用途。

公开(公告)号：US20090118371A1

公开(公告)日：2009-05-07

申请号：US11995985

申请日：2006-07-20

申请人： Villoo Morawala Patell

发明人： Villoo Morawala Patell

IPC分类号： A61K31/20 ,  C07H21/00 ,  C12N15/64 ,  A61P43/00 ,  A23K3/00 ,  C12N1/15 ,  C12P7/64

CPC分类号： C12N9/0083

摘要： The present invention is directed to an isolated delta-6 desaturase gene from Schizochytrium. It is further directed to the cloning of delta-6 desaturase derived from Schizochytrium in Yeast. The nucleic acid sequence and the amino acid sequences of the delta-6 desaturase are disclosed. Further disclosed are the constructs, vector comprising the gene encoding the enzyme delta-6 desaturase in functional combination with the heterologous regulatory sequences. The novel delta-6 desaturase can be used in a metabolic pathway to convert linoleic acid to gamma linolenic acid (omega-6 pathway). The invention provides the identification, isolation of these novel nucleic acids from Schizochytrium that encode the above-mentioned proteins. The invention specifically exemplifies recombinant yeast cells harboring the vector comprising the delta-6 desaturase gene and by the virtue of the enzyme produced shall be able to produce gamnia-linolenic acid.

摘要翻译： 本发明涉及来自裂殖壶菌的分离的δ-6去饱和酶基因。 进一步涉及在酵母中克隆源自裂殖酵母的δ-6去饱和酶。 公开了δ-6去饱和酶的核酸序列和氨基酸序列。 还公开了构建体，其包含与异源调节序列功能性组合的编码Δ-δ去饱和酶的基因的载体。 新型的δ-6去饱和酶可用于将亚油酸转化为γ-亚麻酸（ω-6途径）的代谢途径。 本发明提供这些新型核酸从编码上述蛋白质的裂殖酵母菌的鉴定，分离。 本发明具体举例说明了携带包含δ-6去饱和酶基因的载体的重组酵母细胞，并且所产生的酶的优点将能够产生游离亚麻酸。

公开(公告)号：US08030543B2

公开(公告)日：2011-10-04

申请号：US12087208

申请日：2006-01-12

申请人： Villoo Morawala Patell ,  Rajyashri Ramakrishna Karur

发明人： Villoo Morawala Patell ,  Rajyashri Ramakrishna Karur

IPC分类号： C12N15/82 ,  C12N15/63 ,  C12N15/00

CPC分类号： C12N15/821 ,  C12N9/92

摘要： The invention describes a highly improved, reproducible and a consistent method of transformation and regeneration that results in obtaining 12-15% transgenic plants. The present invention relates to a method of selecting genetically transformed Sunflower explants based on their ability to utilize Xylose as a sole carbohydrate source. Further disclosed is the nucleic acid sequence of the Xylose Isomerase gene, vector construction for incorporation of the selection marker gene and the process of Agrobacterium Mediated Transformation of target host plant with the vector comprising the gene encoding the enzyme Xylose isomerase under the functional combination of the heterologous regulatory sequences. Also disclosed is the method of selecting the putative transformants post transformation with the said vector that possess a metabolic advantage of utilizing Xylose as a sole carbon source. Increased efficiency of regeneration, better growth and survival has been observed on subjection to the described method of positive selection. The subject invention alleviates the disadvantages of negative selection methods such as the undesired elimination of the transformed cells and the potential environmental harm caused due to the dispersal of the antibiotic and the herbicide resistant genes.

摘要翻译： 本发明描述了高度改进的，可重复的和一致的转化和再生方法，其导致获得12-15％的转基因植物。 本发明涉及一种基于其利用木糖作为唯一碳水化合物来源的能力来选择遗传转化的向日葵外植体的方法。 进一步公开的是，在包含编码酶木糖异构酶的基因的载体的功能组合下，将木糖异构酶基因的核酸序列，掺入选择标记基因的载体构建和农杆菌介导的靶宿主植物转化过程 异源调控序列。 还公开了使用具有利用木糖作为唯一碳源的代谢优势的所述载体选择转化后的推定转化体的方法。 对于所选择的阳性选择方法，观察到提高再生效率，更好的生长和生存。 本发明减轻了阴性选择方法的缺点，例如不希望地消除转化细胞，以及由于抗生素和除草剂抗性基因的分散引起的潜在的环境危害。

公开(公告)号：US20110204222A1

公开(公告)日：2011-08-25

申请号：US13126642

申请日：2009-10-28

申请人： Villoo Morawala Patell ,  Renuka Jain ,  Manohar Shinde ,  Henjarappa Jagadeesh Badamaranahalli

发明人： Villoo Morawala Patell ,  Renuka Jain ,  Manohar Shinde ,  Henjarappa Jagadeesh Badamaranahalli

IPC分类号： H01J49/26

CPC分类号： A61K36/48 ,  G01N2030/8813 ,  G01N30/7233

摘要： The present invention relates to identification and characterization of Phytochemicals and metabolites from Trigonella foenum-graceum extract by Liquid chromatography and Mass spectrometry LC-MS/MS.

摘要翻译： 本发明涉及通过液相色谱和质谱LC-MS / MS鉴定和表征来自Trigonella foenum-graceum提取物的植物化学物质和代谢物。

公开(公告)号：US20090246188A1

公开(公告)日：2009-10-01

申请号：US11914753

申请日：2006-05-31

申请人： Villoo Morawala Patell

发明人： Villoo Morawala Patell

IPC分类号： A61K38/48 ,  C12N15/09 ,  A61P35/00

CPC分类号： C12N9/6459 ,  C12Y304/21069

摘要： The present invention relates to the recombinant method used for the production of soluble form of human tissue plasminogen activator variant. In this variant the threonine at position 103 of the endogenous tissue plasminogen activator is replaced by an asparagine leading to a new glycosylation site. At position 117 of the endogenous tissue plasminogen activator asparagine has been replaced by glutamine, leading to the removal of an N linked glycosylation site. At position 296-299 the amino acids lysine, histidine, arginine, and arginine have been replaced by four alanine amino acids. The invention further relates to the de novo synthesis of the nucleic acid sequence encoding tissue plasminogen activator, transformation of the constructed nucleic acid sequences into competent bacteria and sub-cloning of the same into mammalian expression vectors for the expression of the desired protein. DNA constructs comprising the control elements associated with the gene of interest have been disclosed. The recombinant human tissue plasminogen activator, according to the invention, and the salts and functional derivatives thereof, may comprise the active ingredient of pharmaceutical compositions for treatment of treatment of heart attack and stroke patients. These compositions are yet another aspect of the present invention.

摘要翻译： 本发明涉及用于生产可溶形式的人组织纤溶酶原激活物变体的重组方法。 在该变体中，内源性组织纤溶酶原激活物的位置103处的苏氨酸由导致新糖基化位点的天冬酰胺代替。 在内源性组织纤溶酶原激活物天冬酰胺的位置117已被谷氨酰胺取代，导致N-连接的糖基化位点的去除。 在296-299位，氨基酸赖氨酸，组氨酸，精氨酸和精氨酸已被四个丙氨酸氨基酸取代。 本发明还涉及编码组织纤溶酶原激活剂的核酸序列的从头合成，将构建的核酸序列转化为感受态细菌，并将其亚克隆至用于表达所需蛋白质的哺乳动物表达载体中。 已经公开了包含与感兴趣的基因相关的对照元件的DNA构建体。 根据本发明的重组人组织纤溶酶原激活物及其盐和功能衍生物可以包含用于治疗心脏病发作和中风患者的药物组合物的活性成分。 这些组合物是本发明的另一方面。

公开(公告)号：US20080166432A1

公开(公告)日：2008-07-10

申请号：US10568521

申请日：2003-08-15

申请人： Villoo Morawala Patell ,  Dhruvdev Vyas

发明人： Villoo Morawala Patell ,  Dhruvdev Vyas

IPC分类号： A61K36/00 ,  A61P3/10 ,  A61P9/00 ,  A61P35/00

CPC分类号： A61K36/185

摘要： The invention relates to extracts from Terminalia plant species that are capable of being used in methods for managing diseases such as cardiovascular disease, diabetes, degenerative neurological diseases, cancer, age related diseases like amyloidosis, acute pancreatitis, arthritis, atherosclerosis, cancer, heart diseases, inflammatory bowel disease, myocardial infarction, senile dementia, retinal degeneration and senile cataract; owing to the extracts antioxidation potential.The invention also relates to extracts from Terminalia plant species that are capable of being used in methods for managing various infectious diseases.More particularly, the invention relates to certain extracts from Terminalia arjuna, their uses as antimicrobial and antioxidants agents for the treatment of certain diseases heart disease, diabetes, degenerative neurological diseases, cancer, age related disease like amyloidosis, acute pancreatitis, arthritis, atherosclerosis, cancer, cardiovascular disease, inflammatory bowel disease, myocardial infarction, senile dementia, retinal degeneration and senile cataract in mammals, particularly humans, processes for obtaining them and delivery formats therefore

摘要翻译： 本发明涉及能够用于治疗诸如心血管疾病，糖尿病，退行性神经疾病，癌症，年龄相关疾病如淀粉样变性，急性胰腺炎，关节炎，动脉粥样硬化，癌症，心脏病等疾病的方法中的Terminalia植物物种的提取物 ，炎症性肠病，心肌梗塞，老年性痴呆，视网膜变性和老年性白内障; 由于提取物的抗氧化潜力。 本发明还涉及能够用于管理各种感染性疾病的方法中的Terminalia植物物种的提取物。 更具体地，本发明涉及来自Terminalia arjuna的某些提取物，它们作为抗微生物剂的用途和用于治疗某些疾病的疾病心脏病，糖尿病，退行性神经疾病，癌症，与年龄相关的疾病如淀粉样变性，急性胰腺炎，关节炎，动脉粥样硬化， 癌症，心血管疾病，炎性肠病，心肌梗塞，老年性痴呆，哺乳动物，特别是人类的视网膜变性和老年性白内障，因此获得它们的方法和递送格式

公开(公告)号：US20110064833A1

公开(公告)日：2011-03-17

申请号：US12740682

申请日：2007-12-11

申请人： Villoo Morawala Patell ,  Jagadeesh Badamaranahalli Henjarappa ,  Chandramohan Bangalore Siddaiah ,  Rajesh Ullant

发明人： Villoo Morawala Patell ,  Jagadeesh Badamaranahalli Henjarappa ,  Chandramohan Bangalore Siddaiah ,  Rajesh Ullant

IPC分类号： A61K36/61 ,  A61P3/10

CPC分类号： A61K36/54

摘要： The present invention relates to a synergistic herbal composition for diabetes and related disorders comprising extracts of plant Eugenia of concentration ranging between 10-80% and plant Cinnamomum of concentration ranging between 10-80% optionally along with pharmaceutically acceptable excipients; a method of treating diabetes and related disorders in a subject in need thereof by administering the composition comprising extracts of plant Eugenia of concentration ranging between 10-80% and plant Cinnamomum of concentration ranging between 10-80% optionally along with pharmaceutically acceptable excipients; and a process for preparation of a synergistic herbal composition for diabetes and related disorders, wherein the process comprising steps of: (a) obtaining extracts of Eugenia and Cinnamomum separately using aqueous or organic solvents; and (b) formulating the extracts to arrive at the synergistic composition.

摘要翻译： 本发明涉及用于糖尿病和相关病症的协同草药组合物，其包含浓度范围为10-80％的植物优素酸和范围在10-80％范围内的植物樟脑的任选与药学上可接受的赋形剂; 一种在有需要的受试者中治疗糖尿病和相关疾病的方法，包括浓度范围在10-80％之间的浓度范围为10-80％的植物樟木酸提取物的任选与药学上可接受的赋形剂组合; 以及制备用于糖尿病和相关病症的协同草药组合物的方法，其中所述方法包括以下步骤：（a）分别使用水性或有机溶剂获得优素和樟脑提取物; 和（b）制备提取物以获得协同组合物。

公开(公告)号：US20090317501A1

公开(公告)日：2009-12-24

申请号：US12307269

申请日：2006-12-27

申请人： Villoo Morawala Patell

发明人： Villoo Morawala Patell

IPC分类号： A61K36/15 ,  G01N33/567 ,  A61P19/10

CPC分类号： A61K36/15

摘要： The present invention is concerned with nutritional or pharmaceutical compositions comprising extracts or concentrates of plants and the mixtures thereof belonging to Pinus. sp with specific reference to Pinus pinea. The extracts have been screened and characterized for their activity in the treatment of increased bone resorption and bone formation, osteoporosis in particular. The invention further relates to the use of the extracts as a supplement or a medicament useful in the treatment/alleviation or prevention of diseases or conditions characterized by increased bone resorption and a method of promoting bone growth, maintenance of bone health, comprising the administration of an therapeutically effective amount of the composition containing the extract.

摘要翻译： 本发明涉及包含属于松属的植物的提取物或浓缩物及其混合物的营养或药物组合物。 sp具体参考松属松属。 提取物已被筛选和表征，因为它们在治疗增加的骨吸收和骨形成，特别是骨质疏松症方面的活性。 本发明进一步涉及提取物作为补充剂或药物的用途，其可用于治疗/缓解或预防特征为增加的骨吸收的疾病或病症，以及促进骨生长，维持骨骼健康的方法，包括施用 含有该提取物的组合物的治疗有效量。

公开(公告)号：US20090285795A1

公开(公告)日：2009-11-19

申请号：US11914750

申请日：2006-05-24

申请人： Villoo Morawala Patell

发明人： Villoo Morawala Patell

IPC分类号： A61K39/395 ,  C12P21/04

CPC分类号： C07K16/2887 ,  C07K2317/24

摘要： The present invention relates to the recombinant method used for the production of soluble form of an antibody that binds to CD20 for treatment of patients with relapsed or refractory, low-grade or follicular, CD20-positive, B-cell non-Hodgkin's lymphoma (NHL). The treatment will comprise the use of immunologically active anti-CD20 antibodies; or radiolabeled anti-CD20 antibodies and or cooperative strategies where both labeled and non-labeled antibodies will be used for treatment of NHL. The procedure describes the de novo synthesis of the nucleic acid sequence encoding anti-CD20, transformation of the constructed nucleic acid sequences into competent bacteria and the sub-cloning of the same into mammalian expression vectors for expression of the desired protein. DNA constructs comprising the control elements associated with the gene of interest has been disclosed. The nucleic acid sequence of interest has been codon optimized to permit expression in the suitable mammalian host cells.

摘要翻译： 本发明涉及用于生产结合CD20的抗体可溶形式的重组方法，用于治疗复发性或难治性，低级或滤泡性CD20阳性，B细胞非霍奇金淋巴瘤（NHL）的患者 ）。 治疗将包括使用免疫活性的抗CD20抗体; 或放射性标记的抗CD20抗体和/或协同策略，其中标记和未标记的抗体将用于治疗NHL。 该方法描述了编码抗CD20的核酸序列的从头合成，将构建的核酸序列转化为感受态细菌，并将其亚克隆至用于表达所需蛋白质的哺乳动物表达载体中。 已经公开了包含与感兴趣的基因相关的对照元件的DNA构建体。 感兴趣的核酸序列已被密码子优化，以允许在合适的哺乳动物宿主细胞中表达。