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    NOVEL SGLT INHIBITORS
    1.
    发明申请
    NOVEL SGLT INHIBITORS 有权
    新型SGLT抑制剂

    公开(公告)号：US20140378540A1

    公开(公告)日：2014-12-25

    申请号：US14344628

    申请日：2012-09-12

    申请人： Rajesh Jain ,  Sanjay Trehan ,  Jagattaran Das ,  Gurmeet Kaur Nanda ,  Sastry V. R. S Thungathurthi ,  Nishan Singh ,  Sudhir Kumar Sharma

    发明人： Rajesh Jain ,  Sanjay Trehan ,  Jagattaran Das ,  Gurmeet Kaur Nanda ,  Sastry V. R. S Thungathurthi ,  Nishan Singh ,  Sudhir Kumar Sharma

    IPC分类号： C07D309/10 ,  C07D493/08

    CPC分类号： C07D309/10 ,  C07D493/08 ,  C07H7/04

    摘要： The present invention relates to novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also relates to the processes for the synthesis of novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The present invention also provides pharmaceutical compositions comprising novel compounds of Formula I and methods of treating or preventing one or more conditions or diseases that may be regulated or normalized via inhibition of Sodium Glucose Cotransporter-2 (SGLT-2).

    摘要翻译： 本发明涉及式I的新化合物，其药学上可接受的衍生物，互变异构形式，异构体，多晶型物，前药，代谢物，盐或溶剂化物。 本发明还涉及合成式I的新化合物，其药学上可接受的衍生物，互变异构形式，异构体，多晶型物，前药，代谢物，盐或溶剂合物的方法。 本发明还提供包含式I的新化合物和治疗或预防一种或多种可通过抑制葡萄糖转运蛋白-2（SGLT-2）调节或归一化的病症或疾病的药物组合物。

    MANUFACTURABILITY EVALUATION OF INJECTION MOLDED PLASTIC MODELS USING A CAD BASED DFX EVALUATION SYSTEM
    2.
    发明申请
    MANUFACTURABILITY EVALUATION OF INJECTION MOLDED PLASTIC MODELS USING A CAD BASED DFX EVALUATION SYSTEM 审中-公开
    使用基于CAD的DFX评估系统注射成型塑料模型的制造性评估

    公开(公告)号：US20120271443A1

    公开(公告)日：2012-10-25

    申请号：US13542825

    申请日：2012-07-06

    申请人： Bhaskar SINHA ,  Ashish PATIL ,  Ajay A. DESHPANDE ,  Alpana SHARMA ,  Christine ZUZART ,  Sameer KONDEJKAR ,  Rajesh JAIN ,  Nitin UMAP ,  Rahul RAJADHYAKSHA

    发明人： Bhaskar SINHA ,  Ashish PATIL ,  Ajay A. DESHPANDE ,  Alpana SHARMA ,  Christine ZUZART ,  Sameer KONDEJKAR ,  Rajesh JAIN ,  Nitin UMAP ,  Rahul RAJADHYAKSHA

    IPC分类号： G05B19/4097

    CPC分类号： B29C45/7693 ,  G06F17/50 ,  G06F2217/41

    摘要： A method of automatic manufacturability evaluation of plastic models comprises generation of a likely pulling direction, recognition of common features on plastic parts, and then applying manufacturability rules The manufacturability rules can be specified and customized through user specified rule parameters and depend upon the geometric parameters of the recognized features. A system comprises a user interface for selection and customization of DFX (Design for ‘X’) rules for evaluation of a design. The system includes a user interface integrated with a CAD system for receiving the CAD data and displaying the results to the user. Geometry analysis engines are integrated into the system, for extracting the various features and corresponding parameters required as input to the manufacturability rules. The system further involves extensible interfaces for rules and analysis engines which allows users to write their own customized rules and engines and integrate these into the CAD based DFX evaluation system.

    摘要翻译： 塑料模型的自动可制造性评估方法包括产生可能的拉动方向，识别塑料部件上的共同特征，然后应用可制造性规则可制造性规则可以通过用户指定的规则参数来指定和定制，并且取决于几何参数 公认的功能。 系统包括用于选择和定制用于评估设计的DFX（X设计）规则的用户界面。 该系统包括与CAD系统集成的用于接收CAD数据并将结果显示给用户的用户界面。 几何分析引擎集成到系统中，用于提取作为可制造性规则输入所需的各种功能和相应参数。 该系统还涉及规则和分析引擎的可扩展接口，允许用户编写自己的定制规则和引擎，并将其集成到基于CAD的DFX评估系统中。

    NOVEL ANTIMICROBIALS
    3.
    发明申请
    NOVEL ANTIMICROBIALS 有权
    新的抗生素

    公开(公告)号：US20110245258A1

    公开(公告)日：2011-10-06

    申请号：US13130440

    申请日：2009-11-18

    申请人： Rajesh Jain ,  Sanjay Trehan ,  Jagattaran Das ,  Sandeep Kanwar ,  Sitaram Kumar Magadi ,  Sudhir Kumar Sharma

    发明人： Rajesh Jain ,  Sanjay Trehan ,  Jagattaran Das ,  Sandeep Kanwar ,  Sitaram Kumar Magadi ,  Sudhir Kumar Sharma

    IPC分类号： A61K31/4985 ,  C07D487/04 ,  A61K31/519 ,  A61P31/04 ,  A61P31/16 ,  A61P31/06

    CPC分类号： C07D487/04 ,  C07D263/20 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12

    摘要： The present invention relates to novel phenyl oxazolidinone compounds of formula I, their pharmaceutically acceptable analogs, tautomeric forms, stereoisomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also relates to the processes for the synthesis of novel compounds of formula I or their pharmaceutically acceptable analogs, tautomeric forms, stereoisomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The present invention also provides pharmaceutical compositions comprising novel compounds of formula I and methods of using them. The compounds of the present invention are useful as antimicrobial agents, effective against a number of aerobic and/or anaerobic Gram positive and/or Gram negative pathogens such as multi drug resistant species of Staphylococcus, Streptococcus, Enterococcus, Bacterioides, Clostridia, H. influenza, Moraxella, acid-fast organisms such as Mycobacterium tuberculosis as well as Linezolid resistant species of Staphylococcus and Enterococcus.

    摘要翻译： 本发明涉及式I的新型苯基恶唑烷酮化合物，其药学上可接受的类似物，互变异构形式，立体异构体，多晶型物，前药，代谢物，盐或溶剂化物。 本发明还涉及合成新型式I化合物或其药学上可接受的类似物，互变异构体形式，立体异构体，多晶型物，前药，代谢物，盐或溶剂合物的方法。 本发明还提供了包含新颖的式I化合物和使用它们的方法的药物组合物。 本发明的化合物可用作抗微生物剂，对许多需氧和/或厌氧革兰氏阳性和/或革兰氏阴性病原体有效，如葡萄球菌，链球菌，肠球菌，细菌，梭菌，流感嗜血杆菌 ，莫拉氏菌，耐酸菌，如结核分枝杆菌，以及耐盐霉菌属的霉菌和肠球菌。

    COMBINATION VACCINE WITH WHOLE CELL PERTUSSIS
    5.
    发明申请
    COMBINATION VACCINE WITH WHOLE CELL PERTUSSIS 审中-公开
    具有全细胞毒素的组合疫苗

    公开(公告)号：US20110195087A1

    公开(公告)日：2011-08-11

    申请号：US13125679

    申请日：2009-10-23

    申请人： Rajesh Jain ,  Sukhjeet Singh ,  Lavit Jambu

    发明人： Rajesh Jain ,  Sukhjeet Singh ,  Lavit Jambu

    IPC分类号： A61K39/116 ,  A61P37/04 ,  A61P31/04

    CPC分类号： A61K39/0018 ,  A61K39/05 ,  A61K39/08 ,  A61K39/099 ,  A61K39/102 ,  A61K39/12 ,  A61K39/13 ,  A61K39/292 ,  A61K2039/5252 ,  A61K2039/55505 ,  A61K2039/70 ,  C12N2730/10134 ,  C12N2770/32634 ,  Y02A50/466

    摘要： The present invention relates to a combination vaccine comprising a mixture of antigens for protection against diseases such as diphtheria, tetanus, whole cell pertussis and polio. The present invention also relates to inclusion of one or more antigens in the said combination vaccine, for protection against infections caused by Haemophilus influenzae. Hepatitis virus, and other pathogens, such that administration of the vaccine can simultaneously immunize a subject against more than one pathogen. The invention in particular relates to a fully liquid stable combination vaccine comprising the antigens as indicated above and the methods for manufacturing the same.

    摘要翻译： 本发明涉及包含用于保护白血病，破伤风，全细胞百日咳和脊髓灰质炎等疾病的抗原混合物的组合疫苗。 本发明还涉及在所述组合疫苗中包含一种或多种抗原，以防止流感嗜血杆菌引起的感染。 肝炎病毒和其他病原体，使得疫苗的施用可以同时针对多于一种的病原体免疫受试者。 本发明特别涉及包含上述抗原的完全液体稳定的组合疫苗及其制备方法。

    MODIFIED DOSAGE FORMS OF TACROLIMUS
    7.
    发明申请
    MODIFIED DOSAGE FORMS OF TACROLIMUS 审中-公开
    改良剂量剂型

    公开(公告)号：US20100086592A1

    公开(公告)日：2010-04-08

    申请号：US12530011

    申请日：2008-03-25

    申请人： Amarjit Singh ,  Sarabjit Singh ,  Shivanand Puthli ,  Rajesh Jain

    发明人： Amarjit Singh ,  Sarabjit Singh ,  Shivanand Puthli ,  Rajesh Jain

    IPC分类号： A61K9/24 ,  A61K31/436 ,  A61K9/16

    CPC分类号： A61K9/146 ,  A61K9/1676 ,  A61K9/5078 ,  A61K9/5084 ,  A61K31/436

    摘要： The present invention provides a modified release dosage form of tacrolimus that releases two or more amount of tacrolimus upon oral administration, the first amount of tacrolimus releases from the immediate release dosage unit substantially immediately within 0-2 hours followed by a time interval ranging from about 1-10 hours during which substantially no amount of tacrolimus is released from the dosage form, after which a second amount of tacrolimus is released wherein said second amount is released from the delayed release dosage unit either immediately e.g. within 0-2 hours or over a period of time ranging from about 2-12 hours from its initial release from the delayed release dosage unit. The dosage form may further comprise additional amount of tacrolimus to provide additional pulse of tacrolimus. The dosage forms of tacrolimus exhibit improved bioavailability and reduced flux or fluctuation over existing composition of tacrolimus. A method of preparing the dosage forms is also described.

    摘要翻译： 本发明提供了他克莫司的释放剂量形式，其口服给药释放两种或更多量的他克莫司，第一批量的他克莫司基本上立即在0-2小时内立即从即时释放剂量单位释放，之后是从约 1-10小时，其中基本上没有量的他克莫司从剂型中释放出来，之后第二量的他克莫司被释放，其中所述第二量从延迟释放剂量单位释放， 在0-2小时内或超过延迟释放剂量单位从其初始释放约2-12小时的时间段内。 剂型还可包含额外量的他克莫司以提供他克莫司的额外脉冲。 他克莫司的剂型表现出改善的生物利用度和减少通量或波动超过现有组合的他克莫司。 还描述了制备剂型的方法。

    MODIFIED RELEASE PHARMACEUTICAL COMPOSITION AND A PROCESS OF MAKING THE SAME
    8.
    发明申请
    MODIFIED RELEASE PHARMACEUTICAL COMPOSITION AND A PROCESS OF MAKING THE SAME 审中-公开
    改性释放药物组合物及其制备方法

    公开(公告)号：US20100056493A1

    公开(公告)日：2010-03-04

    申请号：US12522185

    申请日：2008-01-24

    申请人： Rajesh Jain ,  Kour Chand Jindal ,  Sanjay Boldhane

    发明人： Rajesh Jain ,  Kour Chand Jindal ,  Sanjay Boldhane

    IPC分类号： A61K31/554 ,  A61K31/5377

    CPC分类号： A61K9/2077

    摘要： The present invention refers to a modified release pharmaceutical composition comprising an in-situ gelling agent (=0.5 % w/w) and a gellation facilitating agent (e.g. calcium sulfate) in an amount of 2-17.5 % w/w. Additionally, the composition contains a release rate controlling polymer such as an acrylate and optionally a pH independent rate controlling polymer such as HPMC. A preferred active agent is mycophenolate mofetil. A process of making the above described composition is also disclosed.

    摘要翻译： 本发明涉及包含2-17.5％w / w的量的原位胶凝剂（= 0.5％w / w）和凝胶促进剂（例如硫酸钙）的改性释放药物组合物。 此外，组合物含有释放速率控制聚合物如丙烯酸酯和任选的pH独立的速率控制聚合物如HPMC。 优选的活性剂是霉酚酸酯。 还公开了制备上述组合物的方法。

    COMPOSITION COMPRISING AT LEAST ONE HIGHER ALIPHATIC ALCOHOL AND AN EXTRACT OF GRIFFONIA SIMPLICIFOLIA
    9.
    发明申请
    COMPOSITION COMPRISING AT LEAST ONE HIGHER ALIPHATIC ALCOHOL AND AN EXTRACT OF GRIFFONIA SIMPLICIFOLIA 失效
    至少包含一种较高的脂肪醇和甘草的提取物的组合物

    公开(公告)号：US20090258896A1

    公开(公告)日：2009-10-15

    申请号：US12299317

    申请日：2007-05-09

    申请人： Rajesh Jain ,  Kour Chand Jindal

    发明人： Rajesh Jain ,  Kour Chand Jindal

    IPC分类号： A61K31/437 ,  A61K31/405 ,  A61P3/10

    CPC分类号： A61K36/48 ,  A61K31/045 ,  A61K36/82 ,  A61K2300/00

    摘要： Novel compositions comprising a combination of at least one higher primary aliphatic alcohol preferably selected from those having 18 to 40 carbon atoms or mixtures thereof, at least one source of 5-hydroxytryptophan (5-HTP) optionally additionally comprising a source of caffeine and/or catechin-polyphenol and/or epigallocatechin gallate as active agents, either alone or in combination with other active agent(s), optionally with one or more excipient(s) are provided. Particularly, the invention relates to compositions and process for preparation of such compositions and method of use thereof for the management of obesity and associated disorders.

    摘要翻译： 包含至少一种优选选自具有18-40个碳原子的高级伯脂肪醇或其混合物的至少一种5-羟基色氨酸（5-HTP）的组合的新型组合物任选地另外包含咖啡因和/或 儿茶素多酚和/或表没食子儿茶素没食子酸酯作为活性剂，单独或与其它活性剂，任选地与一种或多种赋形剂组合使用。 特别地，本发明涉及用于制备这种组合物的组合物和方法及其用于治疗肥胖症和相关疾病的方法。

    Pharmaceutical Compositions Comprising Higher Primary Aliphatic Alcohols and Hmg Coa Reductase Inhibitor and Process of Preparation Thereof
    10.
    发明申请
    Pharmaceutical Compositions Comprising Higher Primary Aliphatic Alcohols and Hmg Coa Reductase Inhibitor and Process of Preparation Thereof 审中-公开
    包含高级初级脂肪醇和Hmg Coa还原酶抑制剂的药物组合物及其制备方法

    公开(公告)号：US20080247962A1

    公开(公告)日：2008-10-09

    申请号：US10586545

    申请日：2005-01-19

    申请人： Rajesh Jain ,  Kour Chand Jindal ,  Sukhjeet Singh

    发明人： Rajesh Jain ,  Kour Chand Jindal ,  Sukhjeet Singh

    IPC分类号： A61K9/12 ,  A61K31/045 ,  A61K31/40 ,  A61P3/00 ,  A61K31/351

    CPC分类号： A61K31/366 ,  A61K31/045 ,  A61K31/40 ,  A61K45/06 ,  A61K2300/00

    摘要： A novel pharmaceutical composition comprising a mixture of higher primary aliphatic alcohols from (24) to (39) carbon atoms; at least one another component selected from resins and pigments, hydrocarbons, esters, ketones and aldehydes, and phenolic compounds, and HMG CoA reductase inhibitor, its salts, analogs or derivatives thereof, preferably statins, optionally with pharmaceutically acceptable excipients, and process of preparation of such composition is provided. Also provided are method of treatment and use of such composition for reducing abnormal lipid parameters associated with hyperlipidemia.

    摘要翻译： 一种新型药物组合物，其包含来自（24）至（39）个碳原子的较高级脂族醇的混合物; 选自树脂和颜料，烃，酯，酮和醛中的至少一种组分和酚类化合物，和HMG CoA还原酶抑制剂，其盐，类似物或衍生物，优选他汀类，任选地具有药学上可接受的赋形剂，以及制备方法 提供了这种组合物。 还提供了治疗和使用这种组合物以减少与高脂血症相关的异常脂质参数的方法。