公开(公告)号：US20100143471A1

公开(公告)日：2010-06-10

申请号：US12528405

申请日：2008-03-17

申请人： Ubaidulla Udhumansha ,  Shirishkumar Kulkarni

发明人： Ubaidulla Udhumansha ,  Shirishkumar Kulkarni

IPC分类号： A61K9/24 ,  A61K31/445 ,  A61P11/02 ,  A61K9/00 ,  A61K9/16 ,  A61P37/08

CPC分类号： A61K9/10 ,  A61K9/1617 ,  A61K9/167 ,  A61K9/1694 ,  A61K9/209 ,  A61K31/137 ,  A61K31/445 ,  A61K2300/00

摘要： A novel reduced dose pharmaceutical composition comprising combination of fexofenadine or salts thereof; and pseudoephedrine or salts thereof in therapeutically effective amount, for the treatment of allergic rhinitis and associated symptoms in pediatric population.

摘要翻译： 一种新型的降低剂量的药物组合物，其包含非索非那定或其盐的组合; 和伪麻黄碱或其盐的治疗有效量，用于治疗儿科人群中的过敏性鼻炎和相关症状。

公开(公告)号：US07691889B2

公开(公告)日：2010-04-06

申请号：US11082947

申请日：2005-03-18

申请人： Sudershan Kumar Arora ,  Vijaykumar Jagdishwar Patil ,  Prathap Sreedharan Nair ,  Prasad Purushottam Dixit ,  Shankar Ajay ,  Rakesh Kumar Sinha

发明人： Sudershan Kumar Arora ,  Vijaykumar Jagdishwar Patil ,  Prathap Sreedharan Nair ,  Prasad Purushottam Dixit ,  Shankar Ajay ,  Rakesh Kumar Sinha

IPC分类号： A61K31/422 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/454 ,  A61K31/496 ,  C07D263/20 ,  C07D413/02 ,  C07D417/02

CPC分类号： C07D263/20 ,  C07D413/10 ,  C07D413/14

摘要： Novel compounds belonging to the class of oxazolidinones possessing potent antimycobacterial properties especially useful in the treatment of acid fast organisms such as Mycobacterium tuberculosis, Mycobacterium avium-intracellular complex, M. fortuitum and M. kansai. The compound and its pharmaceutically acceptable salts act as antibacterial agents. Also mentioned is a method for inhibiting growth of mycobacterial cells as well as a method of treating mycobacterial conditions such as Mycobacterium tuberculosis, drug resistant Mycobacterium tuberculosis, Mycobacterium avium-intracellular complex, M. fortuitum and M. kansai., including administering an antimycobacterially effective amount of the compound and/or pharmaceutically acceptable salts. There is also mentioned a process for the manufacture of the compound or its pharmaceutically acceptable salts.

摘要翻译： 属于恶唑烷酮类的新型化合物具有强效的抗分支杆菌特性，特别适用于治疗结核分枝杆菌，鸟分枝杆菌 - 细胞内复合物，偶然遗传和关西等酸性快速生物。 该化合物及其药学上可接受的盐作为抗菌剂。 还提及了抑制分枝杆菌细胞生长的方法以及治疗结核分枝杆菌，耐药性结核分枝杆菌，鸟分枝杆菌 - 细胞内复合物，偶然和关西的分枝杆菌病症的方法，包括施用抗菌分泌杆菌 化合物和/或其药学上可接受的盐的量。 还提及了制备化合物或其药学上可接受的盐的方法。

公开(公告)号：US07691837B2

公开(公告)日：2010-04-06

申请号：US10497615

申请日：2002-09-20

申请人： Sudershan Kumar Arora ,  Neelima Sinha ,  Sanjay Jain ,  Ram Shankar Upadhayaya ,  Gourhari Jana ,  Shankar Ajay ,  Rakesh Kumar Sinha

发明人： Sudershan Kumar Arora ,  Neelima Sinha ,  Sanjay Jain ,  Ram Shankar Upadhayaya ,  Gourhari Jana ,  Shankar Ajay ,  Rakesh Kumar Sinha

IPC分类号： A01N43/00 ,  A01N43/40 ,  A61K31/33 ,  A61K31/55 ,  A61K31/497 ,  A61K31/435 ,  C07D223/00 ,  C07D243/00 ,  C07D241/04 ,  C07D295/00 ,  C07D213/00

CPC分类号： C07D207/335 ,  C07D207/32 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D417/06

摘要： Novel pyrrole derivatives of formula (I) and their pharmaceutically acceptable acid addition salts having superior antimycobacterial activity against clinically sensitive as well as resistant strains of Mycobacterium tuberculosis as well as having lesser toxicity compared to known compounds. The use of the novel compounds of formula (I) for treatment of latent tuberculosis including Multi Drug Resistant Tuberculosis (MDR TB). The methods for preparation of the novel compounds, pharmaceutical compositions containing the novel compounds and method of treating MDR TB by administration of compounds of formula (I).

公开(公告)号：US20090208575A1

公开(公告)日：2009-08-20

申请号：US11794748

申请日：2006-01-03

申请人： Jyothi Lakshmi Gunupati ,  Suryakumar Jayanthi ,  Himadri Sen

发明人： Jyothi Lakshmi Gunupati ,  Suryakumar Jayanthi ,  Himadri Sen

IPC分类号： A61K9/30 ,  A61K31/4439

CPC分类号： A61K31/133 ,  A61K9/2018 ,  A61K9/2054 ,  A61K9/2059 ,  A61K9/2846 ,  A61K9/2866 ,  A61K9/2886 ,  A61K31/4439 ,  A61K2300/00

摘要： A pharmaceutical composition for oral use comprising a) a core comprising an effective amount of benzimidazole and an organic stabilizing agent which is present in an amount effective to stabilize the composition, b) an intermediate layer comprising of a water insoluble polymer and an organic stabilizer, and c) an outer enteric coating layer. The organic stabilizing agent is present in the core from about 1% to about 10% by weight of the core and in the intermediate layer from about 5% to about 35% by weight of intermediate layer.

摘要翻译： 一种用于口服使用的药物组合物，其包含a）包含有效量的苯并咪唑和有效稳定组合物的有机稳定剂的核心，b）包含水不溶性聚合物和有机稳定剂的中间层， 和c）外肠衣层。 有机稳定剂在核心中以核心的约1重量％至约10重量％存在，中间层中存在约5重量％至约35重量％的中间层。

公开(公告)号：US07482361B2

公开(公告)日：2009-01-27

申请号：US10538858

申请日：2002-12-16

申请人： Girij Pal Singh ,  Govind Singh Rawat ,  Vilas Nathu Dhake ,  Sagar Purshottam Nehate

发明人： Girij Pal Singh ,  Govind Singh Rawat ,  Vilas Nathu Dhake ,  Sagar Purshottam Nehate

IPC分类号： C07D217/06 ,  A61K31/47

CPC分类号： C07D217/26

摘要： A novel crystalline form of quinapril hydrochloride of formula (I) An amorphous form of quinapril hydrochloride substantially free of impurities, specially diketopiperazine compound, and conforming to pharmacopoeial specifications formed from the said novel crystalline form of quinapril hydrochloride of formula (I). The crystalline quinapril hydrochloride is in the form nitroalkane solvate in which the nitroalkane is nitromethane, nitroethane and nitropropanae. Each such nitroalkane solvate having particular characteristic X-ray diffraction patterns. A process for preparation of amorphous form of quinapril hydrochloride, substantially free of impurities, specially diketopiperazine compound, and conforming to pharmacopoeial specifications, using the novel crystalline quinapril hydrochloride as an intermediate. The process involves obtaining free base compound of formula (V) by adjusting the pH of a solution of the benzyl ester maleate salt of quinapril of formula (V) between 7.5-8.5 in a mixture of water and an organic solvent; catalytic hydrogenation of this compound (V) in an alcoholic solvent in the presence of concentrated hydrochloric acid or hydrogen chloride dissolved in an alcoholic solvent and in the presence of catalytic amounts of Pd/C to obtain a residue containing formula (I); crystallization of the said residue by evaporating the alcoholic solvent from a nitroalkane solvent to give crystalline quinapril hydrochloride, associated with a solvate of the nitroalkane solvent, and drying the crystalline quinapril hydrochloride nitroalkane solvate at a temperature between 40° C. and 45° C. under vacuum to give amorphous quinapril hydrochloride of formula (I).

摘要翻译： 式（I）的喹诺酮盐酸盐的新型结晶形式基本上不含杂质的喹诺酮盐酸盐的无定型形式，特别是二酮哌嗪化合物，并且符合由式（I）的所述新型结晶形式的喹那普利盐酸盐形成的药典规格。 喹诺酮结晶盐酸盐为硝基烷烃溶剂合物，其中硝基烷烃为硝基甲烷，硝基乙烷和硝基丙烷。 每种这样的硝基烷烃溶剂合物具有特定的特征X射线衍射图。 基于喹诺酮盐酸盐的无定形形式，基本上不含杂质，特别是二酮哌嗪化合物，并符合药典规格，使用新型喹诺酮盐酸盐作为中间体的方法。 该方法包括通过在水和有机溶剂的混合物中调节式（V）的喹那普利的马来酸苄酯的溶液在7.5-8.5之间的pH值来获得式（Ⅴ）的游离碱化合物; 在溶于酒精溶剂的浓盐酸或氯化氢存在下，在催化量的Pd / C存在下，在醇溶剂中催化氢化该化合物（V），得到含有式（I）的残基。 通过从硝基烷烃溶剂中蒸发醇溶剂来结晶所述残余物，得到与硝基烷烃溶剂的溶剂化物相关的结晶喹诺酮盐酸盐，并在40℃至45℃的温度下干燥喹诺酮结晶盐酸盐硝基烷烃溶剂合物。 在真空下得到式（I）的无定形喹那普利盐酸盐。

公开(公告)号：US07452990B2

公开(公告)日：2008-11-18

申请号：US10540770

申请日：2002-12-26

申请人： Debashish Datta ,  Muralikrishna Dantu ,  Brijkishore Mishra ,  Pollepeddi Lakshmi Narayana Sharma

发明人： Debashish Datta ,  Muralikrishna Dantu ,  Brijkishore Mishra ,  Pollepeddi Lakshmi Narayana Sharma

IPC分类号： C07D501/22 ,  C07D501/24 ,  C07D501/36 ,  C07D501/46 ,  C07D501/34 ,  C07C305/14

CPC分类号： C07D501/00 ,  C07C303/24 ,  C07C305/00 ,  Y02P20/55

摘要： A novel 4-halo-2-oxyimino-3-oxo butyric acid-N,N-dimethyl formiminium chloride chlorosulfate of formula (I) useful in the preparation of cephalosporin antibiotics wherein X is chlorine or bromine; R is hydrogen, C1-4 alkyl group, an easily removable hydroxyl protective group, —CH2COOR5, or —C(CH3)2COOR5, wherein R5 is hydrogen or an easily hydrolysable ester group. The compound of formula (I) is prepared by reacting 4-halo-2-oxyimino-3-oxobutyric acid of formula (IV1), wherein X, R and R5 are as defined above, with N,N-dimethylformiminium chloride chlorosulphate of formula (VII) in an organic solvent at a temperature ranging from −30° C. to −15° C. The cephalosporins that may be prepared from the intermediate include cefdinir, cefditoren pivoxil, cefepime, cefetamet pivoxil, cefixime, cefmenoxime, cefodizime, cefoselis, cefotaxime, cefpirome, cefpodoxime proxetil, cefquinome, ceftazidime, cefteram pivoxil, ceftiofur, ceftizoxime, ceftriaxone and cefuzonam.

摘要翻译： 用于制备头孢菌素抗生素的式（I）的新的4-卤代-2-氧亚氨基-3-氧代丁酸-N-，N-二甲基氯化亚硫酸盐，其中X是氯或溴; R为氢，C 1-4烷基，易脱除的羟基保护基，-CH 2 COOR 5或-C（CH 3） 其中R 5是氢或易水解的酯基。其中R 5是氢或易水解的酯基。 式（I）化合物通过使式（IV ^{）的4-卤代-2-氧亚氨基-3-氧代丁酸（其中X，R和R 5） 与式（VII）的N，N-二甲基甲酰亚胺氯化硫酸盐在有机溶剂中在-30℃至-15℃的温度范围内。可从中间体制备的头孢菌素包括头孢地尼 头孢匹罗，头孢匹肟，头孢他啶，头孢克肟，头孢匹肟，头孢匹肟，头孢噻肟，头孢噻肟，头孢匹罗，头孢泊肟酯，头孢喹肟，头孢他啶，头孢曲松，头孢噻呋，头孢唑肟，头孢曲松和头孢唑胺。}

公开(公告)号：US20080207912A1

公开(公告)日：2008-08-28

申请号：US12150744

申请日：2008-04-30

申请人： Om Dutt Tyagi ,  Santosh Kumar Richhariya ,  Rajesh Kumar Ramchandra Pawar ,  Yuvaraj Atmaram Chavan

发明人： Om Dutt Tyagi ,  Santosh Kumar Richhariya ,  Rajesh Kumar Ramchandra Pawar ,  Yuvaraj Atmaram Chavan

IPC分类号： C07D277/40

CPC分类号： C07D417/14

摘要： A process for preparation of ceftiofur of formula (I) of high purity and substantially free from impurities is disclosed. The process comprises reacting [2-(2-aminothiazol-4-yl)]-2-syn-methoxyimino acetic acid-2-benzothiazolyl thioester of formula (II), with 7-amino-3-(2-furanylcarbonylthiomethyl)-3-cephem-4-carboxylic acid of formula (III) in the presence of a mixture of an water-immescible inert organic solvent and water and in the presence of a organic base and isolating ceftiofur of formula (1) substantially free of impurities by, d) adding water to the reaction mixture and selectively partitioning the impurities in the organic phase and ceftiofur (I) in the form of a salt with the base in the aqueous phase, e) acidifying the aqueous phase containing ceftiofur (I) in the form of a salt with the base in the presence of a mixture containing a water-miscible and a water-immiscible organic solvent and in the presence of a saturated aqueous solution of an alkali or alkaline earth containing salt, to partition ceftiofur (I) in the organic phase, and f) isolating ceftiofur (I) of high purity and substantially free of impurities by evaporation of the organic solvent or precipitation by addition of a co-solvent.

摘要翻译： 公开了一种制备高纯度且基本上不含杂质的式（I）头孢噻呋的方法。 该方法包括使式（II）的[2-（2-氨基噻唑-4-基）] - 2-顺式 - 甲氧基亚氨基乙酸-2-苯并噻唑基硫代酯与7-氨基-3-（2-呋喃基羰硫基甲基）-3 （III）的头孢-4-羧酸在水不溶性惰性有机溶剂和水的混合物存在下，在有机碱的存在下，分离基本上不含杂质的式（1）的头孢噻肟， d）向反应混合物中加入水，并在水相中选择性地分配有机相中的杂质和与碱的盐形式的头孢噻呋（I），e）以含有头孢噻呋（I）的形式酸化含有头孢噻呋 在含有水混溶性和与水不混溶的有机溶剂的混合物存在下，在含有碱或碱土金属盐的饱和水溶液的存在下，将碱与碱反应，从而将头孢噻吩（I） 有机相，和f）分离高纯度和实质的头孢噻呋（I） 通过蒸发有机溶剂或通过加入共溶剂沉淀而不含杂质。

公开(公告)号：US20080102134A1

公开(公告)日：2008-05-01

申请号：US11870744

申请日：2007-10-11

申请人： Dhanashree Mistry ,  Dhananjay Panigrahi ,  T. Kumar ,  Himadri Sen

发明人： Dhanashree Mistry ,  Dhananjay Panigrahi ,  T. Kumar ,  Himadri Sen

IPC分类号： A61K9/16 ,  A61K31/404 ,  A61K47/38

CPC分类号： A61K31/405 ,  A61K9/1652 ,  A61K9/2077 ,  A61K9/2866

摘要： A color stable controlled release pharmaceutical dosage form comprising HMG CoA reductase inhibitor, rate controlling polymers and one or more pharmaceutical excipients wherein the granules are independent of particle size the pharmaceutical dosage form is free of alkalizing/buffering agents. A color stable controlled release pharmaceutical dosage form comprising Fluvastatin Sodium, hydroxypropyl methylcellulose polymer and hydroxypropyl cellulose, wherein the granules are independent of particle size.

摘要翻译： 包含HMG CoA还原酶抑制剂，速率控制聚合物和一种或多种药物赋形剂的颜色稳定的控释药物剂型，其中所述颗粒与颗粒大小无关，药物剂型不含碱化/缓冲剂。 包含氟伐他汀钠，羟丙基甲基纤维素聚合物和羟丙基纤维素的颜色稳定的控释药物剂型，其中颗粒独立于粒度。

公开(公告)号：US07064198B2

公开(公告)日：2006-06-20

申请号：US10468584

申请日：2001-07-25

申请人： Vinod Kumar Kansal ,  Sunil Gurudatt Bhat ,  Tanguturi Venkata Marutikumar ,  Yuvaraj Atmaram Chavan ,  Ramanathan Sankaran

发明人： Vinod Kumar Kansal ,  Sunil Gurudatt Bhat ,  Tanguturi Venkata Marutikumar ,  Yuvaraj Atmaram Chavan ,  Ramanathan Sankaran

IPC分类号： C07D501/34 ,  C07D501/04

CPC分类号： C07D501/00

摘要： A process for preparation of cefuroxime axetil of formula (I) of at least 96% purity and substantially free of analogous Δ2-isomer of formula (II) and other impurities. The process comprises reacting cefuroxime acid of formula (III) with (R,S)-1-acetoxyethyl bromide of formula (IV), and a Group I or II metal carbonate in the presence of a compound of formula (V), MmHnPqOr  (V) wherein M is Group I or II metal; m is 1, 2, 3; n is 0, 1, 2, or 4; q is 1 or 2; r is 4, 7 or 8; in the presence of a C1-4 alcohol and a polar tertiary amide solvent selected from N,N-dimethylacetamide, N,N-dimethylformamide, N,N-dimetheylpropionamide, N,N-diethylacetamide, N,N-diethylformamide and N,N-diethylpropionamide at a temperature ranging from about −30 to +30° C. and subjecting the product thus obtained to a desired step of purification.

摘要翻译： 制备具有至少96％纯度且基本上不含式（II）的类似的三异构体和其它杂质的式（I）头孢呋辛酯的方法。 该方法包括使式（III）的头孢呋辛酸与式（IV）的（R，S）-1-乙酰氧基乙基溴和I或II族金属碳酸盐在式（Ⅴ）化合物存在下反应， in-line-formula description =“In-line Formulas”end =“lead”？> M＆lt;＆lt;＆lt; n＆gt;＆lt;＆lt;＆lt; （V）<？in-line-formula description =“In-line Formulas”end =“tail”？>其中M是I或II族金属; m为1,2,3; n为0,1,2或4; q为1或2; r为4,7或8; 在C 1-4醇和极性叔胺溶剂的存在下，选自N，N-二甲基乙酰胺，N，N-二甲基甲酰胺，N，N-二甲酰基丙酰胺，N，N-二乙基乙酰胺，N ，N-二乙基甲酰胺和N，N-二乙基丙酰胺，温度范围为约-30至+ 30℃，并将所得产物经过所需的纯化步骤。

公开(公告)号：US20050084455A1

公开(公告)日：2005-04-21

申请号：US10685567

申请日：2003-10-16

申请人： Himadri Sen ,  Suryakumar Jayanthi ,  Rakesh Sinha ,  Rolee Sharma ,  Pawan Muttil

发明人： Himadri Sen ,  Suryakumar Jayanthi ,  Rakesh Sinha ,  Rolee Sharma ,  Pawan Muttil

IPC分类号： A61K9/00 ,  A61K9/16 ,  A61K31/00 ,  A61K31/445 ,  A61K31/455 ,  A61L9/04 ,  A61K9/14 ,  A61K31/496

CPC分类号： A61K9/0075 ,  A61K9/0053 ,  A61K9/1647 ,  A61K31/00 ,  A61K31/445 ,  A61K31/455

摘要： The present invention relates to a biodegradable microparticle composition useful for the target specific drug delivery to manage pulmonary tuberculosis, said composition comprising two anti-tuberculosis drugs, and a biodegradable polymer for drug delivery in a ratio of about 1:2 to 2:1, wherein the anti-tubercular drugs are in the ratio of 1:2 to 2:1, also, a process for the preparation of the composition, and lastly, a method of treating pulmonary tuberculosis in a subject, said method comprising administering by inhalation alone or in combination with oral route, pharmaceutically effective amount of the composition to the subject in need thereof, wherein the dosage for inhalation is ranging between 0.5 to 10 mg/kg body weight/day and that for oral route is ranging between 4 to 32 mg/kg body weight/day.

摘要翻译： 本发明涉及可用于目标特异性药物递送以管理肺结核的可生物降解的微粒组合物，所述组合物包含两种抗结核药物和用于药物递送的生物可降解聚合物，其比例为约1:2至2:1， 其中抗结核药物的比例为1:2至2:1，也是制备组合物的方法，最后是治疗受试者肺结核的方法，所述方法包括单独给药 或与口服途径组合的药物有效量的组合物与有需要的受试者组合，其中吸入剂量为0.5至10mg / kg体重/天，口服途径的范围为4至32mg / kg体重/天。