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1. 发明申请

WO2010083537A3 OPTIMAL BIOLOGICAL MARKER FOR THE BIOLOGICAL POTENCY OF EMBLICA OFFICINALIS GAERTN. (AMLA) FRUIT-METHODS AND PRODUCTS THEREOF 审中-公开
标题翻译：最佳生物标志物对于EMBLICA OFFICINALIS GAERTN的生物学意义。（AMLA）水果 - 其方法和产品
公开(公告)号：WO2010083537A3
公开(公告)日：2010-09-23
申请号：PCT/US2010027267
申请日：2010-03-14
申请人： SAMI LABS LTD , MAJEED MUHAMMED , BHAT BEENA , JADHAV ATUL , SRIVASTAVA JYOTISH , NAGABHUSHANAM KALYANAM
发明人： MAJEED MUHAMMED , BHAT BEENA , JADHAV ATUL , SRIVASTAVA JYOTISH , NAGABHUSHANAM KALYANAM
IPC分类号： A61K31/70
CPC分类号： A61K31/7004 , A61K8/602 , A61K8/97 , A61K36/47 , A61K2800/522 , A61Q19/00 , C07H13/08
摘要： Disclosed is the most optimal biomarker for the BIOLOGICAL POTENCY of Emblica Officinalis Gaertn. (AmIa) fruit and products standardized for 5% and above w/w of the said biomarker. Further, the products described herein contain from about 0.0001 0 % to about 4% of free ascorbic acid depending on the raw material used. The optimal biomarker for amla described herein above is represented by STR#1.
摘要翻译：披露的是最有效的生物标志物。（Amia）水果和产品标准化为所述生物标志物的5％及以上w / w。此外，根据所使用的原料，本文所述的产品含有约0.0001％至约4％的游离抗坏血酸。上文描述的amla的最佳生物标志物由STR＃1表示。

2. 发明申请

WO2005065046A2 AN EFFICIENT INDUSTRIAL PROCESS FOR 3-HYDROXY-3-(3’-SULFAMYL-4’-CHLOROPHENYL)PHTALIMIDINE 审中-公开
标题翻译： 3-羟基-3-（3'-磺酰基-4'-氯苯基）苯并咪唑的有效工业方法
公开(公告)号：WO2005065046A2
公开(公告)日：2005-07-21
申请号：PCT/IN2004/000370
申请日：2004-11-30
申请人： IPCA LABORATORIES LIMITED , KUMAR, Ashok , SINGH, Dharmendra , JADHAV, Atul , PANDYA, Darpan, Navinchandra
发明人： KUMAR, Ashok , SINGH, Dharmendra , JADHAV, Atul , PANDYA, Darpan, Navinchandra
CPC分类号： C07D209/48
摘要： The oximination/cyclization of 2-(4-chlorobenzoyl)benzoic acid with hydroxylamine hydrochloride in presence of molar quantities of inorganic base in water or in alcoholic solvents to form 4-(4’-chlorophenyl)-5,6-bent-oxazine-l-one Formula (8) in high yield and purity; reduction of latter with zinc metal and acetic acid to the corresponding phtalimidine of Formula (9); followed by conversion into 2-(3’-chlorosulphonyl-4’-chlorophenyl)phtalimidine Formula (10) by reaction with chlorosulphonic acid and thionyl chloride in the absence of solvent. Amidation of compound of formula (10) was carried out with ammonia gas/solution in non.-aqueous solvent like ketones and polar aprotic solvents like dimethylformamide, to yield compound of formula (11). Oxidation of Formula (11) with hydrogen peroxide in presence of alkali results in high yield of chlorihalidone.
摘要翻译：在水或醇溶剂中存在无机碱的摩尔量存在下，将2-（4-氯苯甲酰基）苯甲酸与羟胺盐酸盐进行肟化/环化，形成4-（4'-氯苯基）-5,6-弯 - 恶嗪 - （8）高产纯度; 用锌金属和乙酸将后者还原成相应的式（9）的对甲苯胺; 然后在不存在溶剂的情况下通过与氯磺酸和亚硫酰氯反应转化为2-（3'-氯磺酰基-4'-氯苯基）苯并咪唑配方（10）。式（10）化合物的酰胺化用氨水/溶液在非水溶剂如酮和极性非质子溶剂如二甲基甲酰胺中进行，得到式（11）的化合物。在碱存在下用过氧化氢氧化式（11）导致氯代吡喃酮的高产率。

3. 发明申请

WO2005062723A2 AN IMPROVED PROCESS FOR THE PREPARATION OF 7-CHLORO-4-(5-N-EHTYL-N-2-HYDROXYETHYLAMINE)-2-PENTYL] AMINOQUINOLINE AND ITS INTERMEDIATES 审中-公开
标题翻译：制备7-氯代-4-（5-N-羟基-2-羟基乙酰胺）-2-戊基]氨基喹啉及其中间体的改进方法
公开(公告)号：WO2005062723A2
公开(公告)日：2005-07-14
申请号：PCT/IN2004/000364
申请日：2004-11-23
申请人： IPCA LABORATORIES LIMITED , KUMAR, Ashok , VYAS, Ketan, Dhansukhlal , SINGH, Dharmendra , NANDAVADEKAR, Sanjay , BHISE, Sanjay , JADHAV, Atul
发明人： KUMAR, Ashok , VYAS, Ketan, Dhansukhlal , SINGH, Dharmendra , NANDAVADEKAR, Sanjay , BHISE, Sanjay , JADHAV, Atul
CPC分类号： C07D215/46
摘要： Disclosed herein is an improved process for the preparation of 7-chloro-4-[5-(N-ethyl-N-2-hydroxyethylamino)-2-pentyl]aminoquinoline comprising of condensation reaction of 4,7 - dichloro quinoline with 5-(n-ethyl-N-2-hydroxyethyl amino)-2-pentylamine and its intermediates which comprises the reaction of protected 1-chloro-4-pentanone with substituted amine followed by deprotection of ketogroup and reductive amination yielding 5-(N-ethyl-N-2-hydroxyethyl amino)-2-pentylamine or 5 - (N,N-diethylamino) - 2 - pentylamine.
摘要翻译：本文公开了一种制备7-氯-4- [5-（N-乙基-N-2-羟乙基氨基）-2-戊基]氨基喹啉的改进方法，其包括4,7-二氯喹啉与5- （n-乙基-N-2-羟乙基氨基）-2-戊胺及其中间体，其包括保护的1-氯-4-戊酮与取代的胺的反应，然后脱酮保护酮基并还原胺化得到5-（N-乙基 -N-2-羟乙基氨基）-2-戊胺或5-（N，N-二乙基氨基）-2-戊胺。

4. 发明申请

WO2010083537A2 OPTIMAL BIOLOGICAL MARKER FOR THE BIOLOGICAL POTENCY OF EMBLICA OFFICINALIS GAERTN. (AMLA) FRUIT-METHODS AND PRODUCTS THEREOF 审中-公开
标题翻译：大学生生物能力的最佳生物标志物。（AMLA）水果方法及其产品
公开(公告)号：WO2010083537A2
公开(公告)日：2010-07-22
申请号：PCT/US2010/027267
申请日：2010-03-14
申请人： SAMI LABS LIMITED , MAJEED, Muhammed , BHAT, Beena , JADHAV, Atul , SRIVASTAVA, Jyotish , NAGABHUSHANAM, Kalyanam
发明人： MAJEED, Muhammed , BHAT, Beena , JADHAV, Atul , SRIVASTAVA, Jyotish , NAGABHUSHANAM, Kalyanam
IPC分类号： A61K31/7012 , A61P25/28 , C07H15/18
CPC分类号： A61K31/7004 , A61K8/602 , A61K8/97 , A61K36/47 , A61K2800/522 , A61Q19/00 , C07H13/08
摘要： Disclosed is the most optimal biomarker for the BIOLOGICAL POTENCY of Emblica Officinalis Gaertn. (AmIa) fruit and products standardized for 5% and above w/w of the said biomarker. Further, the products described herein contain from about 0.0001 0 % to about 4% of free ascorbic acid depending on the raw material used. The optimal biomarker for amla described herein above is represented by STR#1.
摘要翻译：公开了用于Emblica Officinalis Gaertn.AmIa果实的生物学潜力的最佳生物标志物和标准化所述生物标志物的5％w / w以上的产品。此外，取决于所使用的原料，本文所述的产品含有约0.0001％至约4％的游离抗坏血酸。以上描述的amla的最佳生物标志物由STR＃1表示。

5. 发明申请

WO2005065046A3 AN EFFICIENT INDUSTRIAL PROCESS FOR 3-HYDROXY-3-(3'-SULFAMYL-4'-CHLOROPHENYL)PHTALIMIDINE 审中-公开
标题翻译： 3-羟基-3-（3'-磺酰基-4'-氯苯基）苯并咪唑的有效工业方法
公开(公告)号：WO2005065046A3
公开(公告)日：2006-08-17
申请号：PCT/IN2004000370
申请日：2004-11-30
申请人： IPCA LAB LTD , KUMAR ASHOK , SINGH DHARMENDRA , JADHAV ATUL , PANDYA DARPAN NAVINCHANDRA
发明人： KUMAR ASHOK , SINGH DHARMENDRA , JADHAV ATUL , PANDYA DARPAN NAVINCHANDRA
IPC分类号： C07D209/44
CPC分类号： C07D209/48
摘要： The oximination/cyclization of 2-(4-chlorobenzoyl)benzoic acid with hydroxylamine hydrochloride in presence of molar quantities of inorganic base in water or in alcoholic solvents to form 4-(4'-chlorophenyl)-5,6-bent-oxazine-l-one Formula (8) in high yield and purity; reduction of latter with zinc metal and acetic acid to the corresponding phtalimidine of Formula (9); followed by conversion into 2-(3'-chlorosulphonyl-4'-chlorophenyl)phtalimidine Formula (10) by reaction with chlorosulphonic acid and thionyl chloride in the absence of solvent. Amidation of compound of formula (10) was carried out with ammonia gas/solution in non.-aqueous solvent like ketones and polar aprotic solvents like dimethylformamide, to yield compound of formula (11). Oxidation of Formula (11) with hydrogen peroxide in presence of alkali results in high yield of chlorihalidone.
摘要翻译：在水或醇溶剂中存在无机碱的摩尔量存在下，将2-（4-氯苯甲酰基）苯甲酸与羟胺盐酸盐进行肟化/环化，形成4-（4'-氯苯基）-5,6-弯 - 恶嗪 - （8）高产纯度; 用锌金属和乙酸将后者还原成相应的式（9）的对甲苯胺; 然后在不存在溶剂的情况下通过与氯磺酸和亚硫酰氯反应转化为2-（3'-氯磺酰基-4'-氯苯基）苯并咪唑配方（10）。式（10）化合物的酰胺化用氨水/溶液在非水溶剂如酮和极性非质子溶剂如二甲基甲酰胺中进行，得到式（11）的化合物。在碱存在下用过氧化氢氧化式（11）导致氯代吡喃酮的高产率。

6. 发明申请

WO2006046253A1 A ONE-POT PROCESS FOR THE PREPARATION OF ANTIEMETIC AGENT, 1,2,3,9-TETRAHYDRO-9-METHYL-3[(2-METHYL)-1H-IMIDAZOLE-1-YL)METHYL]-4H-CARBAZOL-4-O 审中-公开
标题翻译： 1,9-四氢-9-甲基-3 [（2-甲基）-1H-咪唑-1-基）甲基] -4H-卡巴唑-4的制备方法1制备方法 -O
公开(公告)号：WO2006046253A1
公开(公告)日：2006-05-04
申请号：PCT/IN2004/000336
申请日：2004-10-26
申请人： IPCA LABORATORIES LIMITED , KUMAR, Ashok , SINGH, Dharmendra , JADHAV, Atul , PANDYA, Darpan, Navinchandra , PANMAND, Deepak, Shankar , THAKUR, Gajendrasingh, Ramsingh
发明人： KUMAR, Ashok , SINGH, Dharmendra , JADHAV, Atul , PANDYA, Darpan, Navinchandra , PANMAND, Deepak, Shankar , THAKUR, Gajendrasingh, Ramsingh
IPC分类号： C07D233/56
CPC分类号： C07D403/06
摘要： A one-pot industrial process for preparing 1,2,3,9-tetrahydro-9-methyl-3-[(2-methyl-1H-imidazole-1-yl)methyl]-4H-carbazol-4-one of Formula-(I) from 1,2,3,9-tetrahydro-9-methyl-4H-carbazol-4-one of Formula-(IV) involves reaction of Formula (IV) with HNR 1 R 2 salt and paraformaldehyde, where R 1 ,R 2 are independently alkyl groups or together forms a cyclic alkyl group, in a solvent system of acetic acid and hydrocarbon solvent to form a crude mixture of intermediate compounds of Formula (III) and (VIII), which is converted to ondansetron (Formula (I)) without isolation by reaction with 2methyimidazole in a suitable solvent system in the same pot.
摘要翻译：制备式为1,2,3,9-四氢-9-甲基-3 - [（2-甲基-1H-咪唑-1-基）甲基] -4H-咔唑-4-酮的一锅工业方法 - （I）由式（Ⅳ）的1,2,3,9-四氢-9-甲基-4H-咔唑-4-酮包括式（Ⅳ）与HNR 1 R 其中R 1，R 2，R 2独立地为烷基或一起形成环烷基，在乙酸的溶剂体系中酸和烃溶剂形成式（III）和（VIII）的中间体化合物的粗制混合物，其在相同的罐中在合适的溶剂体系中与2-甲基咪唑反应而不分离而转化成昂丹司琼（式（I））。

7. 发明申请

WO2005062723A3 AN IMPROVED PROCESS FOR THE PREPARATION OF 7-CHLORO-4-(5-N-EHTYL-N-2-HYDROXYETHYLAMINE)-2-PENTYL] AMINOQUINOLINE AND ITS INTERMEDIATES 审中-公开
标题翻译：制备7-氯代-4-（5-N-羟基-2-羟基乙酰胺）-2-戊基]氨基喹啉及其中间体的改进方法
公开(公告)号：WO2005062723A3
公开(公告)日：2006-01-05
申请号：PCT/IN2004000364
申请日：2004-11-23
申请人： IPCA LAB LTD , KUMAR ASHOK , VYAS KETAN DHANSUKHLAL , SINGH DHARMENDRA , NANDAVADEKAR SANJAY , BHISE SANJAY , JADHAV ATUL
发明人： KUMAR ASHOK , VYAS KETAN DHANSUKHLAL , SINGH DHARMENDRA , NANDAVADEKAR SANJAY , BHISE SANJAY , JADHAV ATUL
IPC分类号： C07D215/38 , C07D215/44 , C07D215/46
CPC分类号： C07D215/46
摘要： Disclosed herein is an improved process for the preparation of 7-chloro-4-[5-(N-ethyl-N-2-hydroxyethylamino)-2-pentyl]aminoquinoline comprising of condensation reaction of 4,7 - dichloro quinoline with 5-(n-ethyl-N-2-hydroxyethyl amino)-2-pentylamine and its intermediates which comprises the reaction of protected 1-chloro-4-pentanone with substituted amine followed by deprotection of ketogroup and reductive amination yielding 5-(N-ethyl-N-2-hydroxyethyl amino)-2-pentylamine or 5 - (N,N-diethylamino) - 2 - pentylamine.
摘要翻译：本文公开了一种制备7-氯-4- [5-（N-乙基-N-2-羟乙基氨基）-2-戊基]氨基喹啉的改进方法，其包括4,7-二氯喹啉与5- （n-乙基-N-2-羟乙基氨基）-2-戊胺及其中间体，其包括保护的1-氯-4-戊酮与取代的胺的反应，然后脱酮保护酮基并还原胺化得到5-（N-乙基 -N-2-羟乙基氨基）-2-戊胺或5-（N，N-二乙基氨基）-2-戊胺。

8. 发明申请

WO2004092142A1 AN IMPROVED PROCESS FOR MANUFACTURE OF SUBSTITUTED BENZIMIDAZOLES 审中-公开
标题翻译：改进的取代苄基咪唑的改进方法
公开(公告)号：WO2004092142A1
公开(公告)日：2004-10-28
申请号：PCT/IN2003/000314
申请日：2003-09-17
申请人： IPCA LABORATORIES LIMITED , VYAS, Ketan, Dhansukhal , SINGH, Dharmendra , NANDAVADEKAR, Sanjay , BHISE, Sanjay , JADHAV, Atul , DESAI, Hemal
发明人： VYAS, Ketan, Dhansukhal , SINGH, Dharmendra , NANDAVADEKAR, Sanjay , BHISE, Sanjay , JADHAV, Atul , DESAI, Hemal
IPC分类号： C07D235/28
CPC分类号： C07D235/28
摘要： The present invention relates to a process for the production of benzimidazole derivatives comprising providing an amino acetamido benzene derivative; and condensing and cyclising the aminoacetamido benzene derivative in the presence of a base and in the presence of a cyclising agent under conditions effective to form the benzimidazole derivative. The acetamido benzene derivative has the formula (I) wherein R is OMe or OCHF 2 . The resulting substituted benzimidazoles are key intermediates in the synthesis of H + /K + -ATPase irreversible inhibitors, most particularly Omeprazole.
摘要翻译：本发明涉及生产苯并咪唑衍生物的方法，包括提供氨基乙酰氨基苯衍生物; 并在碱的存在下和在有效形成苯并咪唑衍生物的条件下在环化剂存在下缩合和环化氨基乙酰胺基苯衍生物。乙酰氨基苯衍生物具有式（I），其中R是OMe或OCHF 2。所得取代的苯并咪唑是合成H + / K + - ATP酶不可逆抑制剂，最特别是奥美拉唑的关键中间体。

9. 发明申请

WO2010083537A8 OPTIMAL BIOLOGICAL MARKER FOR THE BIOLOGICAL POTENCY OF EMBLICA OFFICINALIS GAERTN. (AMLA) FRUIT-METHODS AND PRODUCTS THEREOF 审中-公开
标题翻译：最佳生物标志物对于EMBLICA OFFICINALIS GAERTN的生物学意义。（AMLA）水果 - 其方法和产品
公开(公告)号：WO2010083537A8
公开(公告)日：2011-09-01
申请号：PCT/US2010027267
申请日：2010-03-14
申请人： SAMI LABS LTD , MAJEED MUHAMMED , BHAT BEENA , JADHAV ATUL , SRIVASTAVA JYOTISH , NAGABHUSHANAM KALYANAM
发明人： MAJEED MUHAMMED , BHAT BEENA , JADHAV ATUL , SRIVASTAVA JYOTISH , NAGABHUSHANAM KALYANAM
IPC分类号： A61K31/70
CPC分类号： A61K31/7004 , A61K8/602 , A61K8/97 , A61K36/47 , A61K2800/522 , A61Q19/00 , C07H13/08
摘要： Disclosed is the most optimal biomarker for the BIOLOGICAL POTENCY of Emblica Officinalis Gaertn. (AmIa) fruit and products standardized for 5% and above w/w of the said biomarker. Further, the products described herein contain from about 0.0001 0 % to about 4% of free ascorbic acid depending on the raw material used. The optimal biomarker for amla described herein above is represented by STR#1.
摘要翻译：披露的是最有效的生物标志物。（Amia）水果和产品标准化为所述生物标志物的5％及以上w / w。此外，根据所使用的原料，本文所述的产品含有约0.0001％至约4％的游离抗坏血酸。上文描述的amla的最佳生物标志物由STR＃1表示。

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