公开(公告)号：US08741932B2

公开(公告)日：2014-06-03

申请号：US13508135

申请日：2010-11-04

申请人： Sanjay Kumar ,  Sivaramakrishnan Hariharan ,  Mandar Bhonde ,  Nilesh Dagia ,  Rajiv Sharma ,  Pallavi Hanmantrao Mane ,  Pramod Bhaskar Kumar

发明人： Sanjay Kumar ,  Sivaramakrishnan Hariharan ,  Mandar Bhonde ,  Nilesh Dagia ,  Rajiv Sharma ,  Pallavi Hanmantrao Mane ,  Pramod Bhaskar Kumar

IPC分类号： A01N43/40 ,  A61K31/44 ,  A01N43/54 ,  A61K31/535 ,  C07D491/02 ,  C07D265/36 ,  C07D498/02 ,  C07D413/00

CPC分类号： C07D471/04

摘要： The present invention relates to compounds of formula (I), wherein Ra, Rb, Rc, Rd, Re and Rf 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 (PI3K), 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（PI3K），雷帕霉素的哺乳动物靶（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。

公开(公告)号：US20110312970A1

公开(公告)日：2011-12-22

申请号：US13222662

申请日：2011-08-31

申请人： Nabajyoti DEKA ,  Sivaramakrishnan HARIHARAN ,  Swapnil Ramesh BAJARE ,  Rosalind Adaikalasamy MARITA

发明人： Nabajyoti DEKA ,  Sivaramakrishnan HARIHARAN ,  Swapnil Ramesh BAJARE ,  Rosalind Adaikalasamy MARITA

IPC分类号： A61K31/496 ,  A61P5/50 ,  A61P3/10 ,  A61P3/04 ,  A61P1/16 ,  A61P9/10 ,  A61P15/00 ,  A61P7/00 ,  A61P9/12 ,  A61K31/4439 ,  A61P3/06

CPC分类号： C07D401/12

摘要： The present invention provides novel compounds represented by the general formula (I): their stereoisomers, pharmaceutically acceptable salts and their pharmaceutically acceptable solvates thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia. The invention also relates to a process for the manufacture of compounds of formula (I) and pharmaceutical compositions containing them.

摘要翻译： 本发明提供由通式（I）表示的新型化合物：其立体异构体，药学上可接受的盐及其药学上可接受的溶剂化物，其可用于治疗与胰岛素抵抗或高血糖相关的代谢紊乱。 本发明还涉及制备式（I）化合物和含有它们的药物组合物的方法。

公开(公告)号：US20090247574A1

公开(公告)日：2009-10-01

申请号：US12441891

申请日：2007-09-20

申请人： Nabajyoti Deka ,  Kamlesh Jyotindra Padiya ,  Swapnil Ramesh Bajare ,  Rhushikesh Arun Kulkarni ,  Taj Usman Khan ,  Sivaramakrishnan Hariharan ,  Rosalind Adaikalasamy Marita

发明人： Nabajyoti Deka ,  Kamlesh Jyotindra Padiya ,  Swapnil Ramesh Bajare ,  Rhushikesh Arun Kulkarni ,  Taj Usman Khan ,  Sivaramakrishnan Hariharan ,  Rosalind Adaikalasamy Marita

IPC分类号： A61K31/4725 ,  C07D401/02 ,  A61K31/4709

CPC分类号： C07D401/12

摘要： The present invention provides novel compounds represented by the general formula (I): their pharmaceutically acceptable salts and their pharmaceutically acceptable solvates thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia. The invention also relates to a process for the manufacture of compounds of formula (I) and pharmaceutical compositions containing them.

摘要翻译： 本发明提供由通式（I）表示的新化合物：其药学上可接受的盐及其药学上可接受的溶剂化物，其可用于治疗与胰岛素抵抗或高血糖相关的代谢紊乱。 本发明还涉及制备式（I）化合物和含有它们的药物组合物的方法。

公开(公告)号：US08697653B2

公开(公告)日：2014-04-15

申请号：US13813470

申请日：2011-08-04

申请人： Geetanjali Chandrashekhar Chimote ,  Girish Badrinath Mahajan ,  Aravindan Vasudevan ,  Sivaramakrishnan Hariharan

发明人： Geetanjali Chandrashekhar Chimote ,  Girish Badrinath Mahajan ,  Aravindan Vasudevan ,  Sivaramakrishnan Hariharan

IPC分类号： A61K38/12

CPC分类号： A61K38/12 ,  A61K9/0078 ,  A61K9/127 ,  A61K31/4745

摘要： The present invention relates to a biodegradable, inhalable microparticle formulation comprising a compound of formula I obtained by fermentation of a microorganism of the Streptomyces species (PM0626271/MTCC5447), as described in PCT application publication WO2011027290, and a biodegradable lipid for drug delivery wherein the ratio of drug (compound of formula I) to lipid is 1:15 to 1:25. The present invention also relates to the process for preparation of the formulation and to the method of treatment of pulmonary tuberculosis, multi drug resistant tuberculosis (MDRTB), methicillin resistant Staphylococcus aureus (MRSA) pneumonias and methicillin sensitive Staphylococcus aureus (MSSA) pneumonias by administering therapeutically effective amount of the formulation to a mammal in need thereof. The present invention further relates to a method of delivering the microparticle formulation to a mammal in need thereof, wherein the formulation is administered by inhalation or intratracheal instillation for pulmonary delivery.

摘要翻译： 本发明涉及一种可生物降解的可吸入微粒制剂，其包含如PCT申请公开WO 2011027290中所述通过发酵Streptomyces物种微生物（PM0626271 / MTCC5447）获得的式I化合物和用于药物递送的可生物降解的脂质，其中 药物（式I化合物）与脂质的比例为1:15至1:25。 本发明还涉及制剂的制备方法和治疗肺结核，多药耐药结核病（MDRTB），耐甲氧西林金黄色葡萄球菌（MRSA）肺炎和甲氧西林敏感性金黄色葡萄球菌（MSSA）肺炎的方法，通过施用 给予有需要的哺乳动物的治疗有效量的制剂。 本发明还涉及将微粒制剂递送至有需要的哺乳动物的方法，其中所述制剂通过吸入或气管内滴注给予肺部输送。

公开(公告)号：US20130125879A1

公开(公告)日：2013-05-23

申请号：US13813470

申请日：2011-08-04

申请人： Geetanjali Chandrashekhar Chimote ,  Girish Badrinath Mahajan ,  Aravindan Vasudevan ,  Sivaramakrishnan Hariharan

发明人： Geetanjali Chandrashekhar Chimote ,  Girish Badrinath Mahajan ,  Aravindan Vasudevan ,  Sivaramakrishnan Hariharan

IPC分类号： A61K38/12

CPC分类号： A61K38/12 ,  A61K9/0078 ,  A61K9/127 ,  A61K31/4745

摘要： The present invention relates to a biodegradable, inhalable microparticle formulation comprising a compound of formula I obtained by fermentation of a microorganism of the Streptomyces species (PM0626271/MTCC5447), as described in PCT application publication WO2011027290, and a biodegradable lipid for drug delivery wherein the ratio of drug (compound of formula I) to lipid is 1:15 to 1:25. The present invention also relates to the process for preparation of the formulation and to the method of treatment of pulmonary tuberculosis, multi drug resistant tuberculosis (MDRTB), methicillin resistant Staphylococcus aureus (MRSA) pneumonias and methicillin sensitive Staphylococcus aureus (MSSA) pneumonias by administering therapeutically effective amount of the formulation to a mammal in need thereof. The present invention further relates to a method of delivering the microparticle formulation to a mammal in need thereof, wherein the formulation is administered by inhalation or intratracheal instillation for pulmonary delivery.

摘要翻译： 本发明涉及一种可生物降解的可吸入微粒制剂，其包含如PCT申请公开WO 2011027290中所述通过发酵Streptomyces物种微生物（PM0626271 / MTCC5447）获得的式I化合物和用于药物递送的可生物降解的脂质，其中 药物（式I化合物）与脂质的比例为1:15至1:25。 本发明还涉及制剂的制备方法和治疗肺结核，多药耐药结核病（MDRTB），耐甲氧西林金黄色葡萄球菌（MRSA）肺炎和甲氧西林敏感性金黄色葡萄球菌（MSSA）肺炎的方法，通过施用 给予有需要的哺乳动物的治疗有效量的制剂。 本发明还涉及将微粒制剂递送至有需要的哺乳动物的方法，其中所述制剂通过吸入或气管内滴注给予肺部输送。

公开(公告)号：US08269010B2

公开(公告)日：2012-09-18

申请号：US12441891

申请日：2007-09-20

申请人： Nabajyoti Deka ,  Kamlesh Jyotindra Padiya ,  Swapnil Ramesh Bajare ,  Rhushikesh Arun Kulkarni ,  Taj Usman Khan ,  Sivaramakrishnan Hariharan ,  Rosalind Adaikalasamy Marita

发明人： Nabajyoti Deka ,  Kamlesh Jyotindra Padiya ,  Swapnil Ramesh Bajare ,  Rhushikesh Arun Kulkarni ,  Taj Usman Khan ,  Sivaramakrishnan Hariharan ,  Rosalind Adaikalasamy Marita

IPC分类号： C07D217/22 ,  A61K31/4725

CPC分类号： C07D401/12

摘要： The present invention provides novel compounds represented by the general formula (I): their pharmaceutically acceptable salts and their pharmaceutically acceptable solvates thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia. The invention also relates to a process for the manufacture of compounds of formula (I) and pharmaceutical compositions containing them.

摘要翻译： 本发明提供由通式（I）表示的新化合物：其药学上可接受的盐及其药学上可接受的溶剂化物，其可用于治疗与胰岛素抵抗或高血糖相关的代谢紊乱。 本发明还涉及制备式（I）化合物和含有它们的药物组合物的方法。

公开(公告)号：US08030324B2

公开(公告)日：2011-10-04

申请号：US12441802

申请日：2007-09-20

申请人： Nabajyoti Deka ,  Sivaramakrishnan Hariharan ,  Swapnil Ramesh Bajare ,  Rosalind Adaikalasamy Marita

发明人： Nabajyoti Deka ,  Sivaramakrishnan Hariharan ,  Swapnil Ramesh Bajare ,  Rosalind Adaikalasamy Marita

IPC分类号： A61K31/435 ,  A61K31/4439 ,  C07D401/02

CPC分类号： C07D401/12

摘要： The present invention provides novel compounds represented by the general formula (I): their stereoisomers, pharmaceutically acceptable salts and their pharmaceutically acceptable solvates thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia. The invention also relates to a process for the manufacture of compounds of formula (I) and pharmaceutical compositions containing them.

摘要翻译： 本发明提供由通式（I）表示的新型化合物：其立体异构体，药学上可接受的盐及其药学上可接受的溶剂化物，其可用于治疗与胰岛素抵抗或高血糖相关的代谢紊乱。 本发明还涉及制备式（I）化合物和含有它们的药物组合物的方法。

公开(公告)号：US20100185020A1

公开(公告)日：2010-07-22

申请号：US12668984

申请日：2008-07-11

申请人： Sivaramakrishnan Hariharan ,  Owen Chambers ,  Abhay Atmaram Upare ,  Damodharan Satagopan

发明人： Sivaramakrishnan Hariharan ,  Owen Chambers ,  Abhay Atmaram Upare ,  Damodharan Satagopan

IPC分类号： C07C41/22

CPC分类号： C07C41/22 ,  C07C43/123

摘要： The present invention provides a continuous process for the production of 1,2,2,2-tetrafluoroethyl difluoromethyl ether (desflurane) which comprises feeding continuously optimum molar quantities of 1-chloro-2,2,2-trifluoroethyl difluoromethyl ether (CF3CHClOCHF2, Isoflurane) and anhydrous hydrogen fluoride, in a reactor in the vapour phase over a fluorination catalyst system comprising a metal pentahalide absorbed on a supporting substrate at a temperature ranging from 100° C. to 180° C., and separating 1,2,2,2-tetrafluoroethyl difluoromethyl ether (desflurane) continuously from the reactor. The process of the present invention enables continuous removal of desflurane product thereby minimizing co-production of byproducts and resulting in high conversion efficiency and yield of desflurane.

摘要翻译： 本发明提供了用于生产1,2,2,2-四氟乙基二氟甲基醚（地氟烷）的连续方法，该方法包括连续进料最佳摩尔量的1-氯-2,2,2-三氟乙基二氟甲基醚（CF 3 CHClOCHF 2，异氟烷 ）和无水氟化氢，在气相中的反应器中，在氟化催化剂体系中，包含在100℃至180℃的温度范围内吸附在支撑基底上的金属五氢化物， 连续从反应器中加入2-四氟乙基二氟甲基醚（地氟烷）。 本发明的方法能够连续除去地氟烷产物，从而最小化副产物的共生产并产生高的转化效率和地氟烷的产率。

公开(公告)号：US20100022554A1

公开(公告)日：2010-01-28

申请号：US12441802

申请日：2007-09-20

申请人： Nabajyoti Deka ,  Sivaramakrishnan Hariharan ,  Swapnil Ramesh Bajare ,  Rosalind Adaikalasamy Marita

发明人： Nabajyoti Deka ,  Sivaramakrishnan Hariharan ,  Swapnil Ramesh Bajare ,  Rosalind Adaikalasamy Marita

IPC分类号： A61K31/497 ,  C07D401/02 ,  A61P3/10 ,  A61K31/4439

CPC分类号： C07D401/12

摘要： The present invention provides novel compounds represented by the general formula (I): their stereoisomers, pharmaceutically acceptable salts and their pharmaceutically acceptable solvates thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia. The invention also relates to a process for the manufacture of compounds of formula (I) and pharmaceutical compositions containing them.

摘要翻译： 本发明提供由通式（I）表示的新型化合物：其立体异构体，药学上可接受的盐及其药学上可接受的溶剂化物，其可用于治疗与胰岛素抵抗或高血糖相关的代谢紊乱。 本发明还涉及制备式（I）化合物和含有它们的药物组合物的方法。

公开(公告)号：US20070123591A1

公开(公告)日：2007-05-31

申请号：US11583953

申请日：2006-10-20

申请人： Nagarajan Kuppuswamy ,  Sivaramakrishnan Hariharan ,  Venkatachalam Sankar Iyer ,  Suresh Babu Balakrishnan ,  Gopalakrishnan Krishnamurthi ,  Ananda Kuppanna ,  Muruga Poopati Raja Karuppiah ,  Balaram Padmanabhan ,  Aravinda Subrayashastry ,  Gouriamma Vasudev Prema ,  Shamala Narayanaswamy

发明人： Nagarajan Kuppuswamy ,  Sivaramakrishnan Hariharan ,  Venkatachalam Sankar Iyer ,  Suresh Babu Balakrishnan ,  Gopalakrishnan Krishnamurthi ,  Ananda Kuppanna ,  Muruga Poopati Raja Karuppiah ,  Balaram Padmanabhan ,  Aravinda Subrayashastry ,  Gouriamma Vasudev Prema ,  Shamala Narayanaswamy

IPC分类号： A61K31/195 ,  C07C229/12

CPC分类号： C07C229/28 ,  C07C233/08 ,  C07C2601/14

摘要： The present invention relates to compounds trans (E) and cis (Z) stereoisomers of 4-t-butyl gabapentin of formula (11) and (12) and a process for the preparation of the said stereoisomers.

摘要翻译： 本发明涉及式（11）和（12）的4-叔丁基加巴喷丁的反式（E）和顺式（Z）立体异构体的制备方法和所述立体异构体的制备方法。