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1. 发明申请

US20020103181A1 Pharmaceutical composition for controlled release of an active ingredient 审中-公开
标题翻译：用于控制释放活性成分的药物组合物
公开(公告)号：US20020103181A1
公开(公告)日：2002-08-01
申请号：US09726636
申请日：2000-11-30
申请人： LUPIN LABORATORIES LIMITED
发明人： Himadri Sen , Rajesh Suresh Kshirsagar , Chandrashekhar Shriram Kandi , Shailesh Suresh Bhamare
IPC分类号： A61K031/545
CPC分类号： A61K31/545 , A61K9/205 , A61K9/209
摘要： A pharmaceutical composition in the form of a tablet for controlled release of an active ingredient comprises a betalactam antibiotic such as cephalexin, cefaclor or their pharmaceutically acceptable hydrates, salts or esters as active ingredient, and a mixture of hydrophilic polymers selected from the group consisting of at least one sodium alginate and at least one xanthan gum as controlled release matrix; and optionally probenecid as an antibiotic adjuvant as either immediate release or controlled release part. The composition may also contain one or more of a water soluble and/or water dispersible diluent, wherein the quantities of the hydrophilic polymers and water soluble and/or water dispersible diluents are such that the therapeutically effective active ingredient is released at a rate suitable for once or twice daily administration of the pharmaceutical composition. Inclusion of probenecid allows reduction in the amount of active incorporated in the hydrophilic polymer matrix but still provides the desired once a day profile. The resulting modified release matrix formulation not containing probenecid may be administered once or twice daily. The resulting modified release matrix formulation containing probenecid may be administered once daily.
摘要翻译：用于控制释放活性成分的片剂形式的药物组合物包括β-内酰胺抗生素如头孢氨苄，头孢克洛或其药学上可接受的水合物，盐或酯作为活性成分，以及选自以下的亲水性聚合物的混合物：至少一种藻酸钠和至少一种黄原胶作为受控释放基质; 和可选地作为抗生素佐剂的丙磺舒作为立即释放或控制释放部分。组合物还可以含有一种或多种水溶性和/或水分散性稀释剂，其中亲水性聚合物和水溶性和/或水分散性稀释剂的量使得治疗有效的活性成分以适合于每天一次或两次给药药物组合物。包含丙磺舒可以减少亲水性聚合物基质中掺入的活性物质，但仍能提供所需的一天一次。不含丙磺舒的所得改性释放基质制剂可以每天施用一次或两次。含有丙磺舒的所得改性释放基质制剂可以每天施用一次。

2. 发明申请

WO2002087547A1 AN IMPROVED PROCESS FOR PREPARATION OF FOUR-DRUG ANTI-TUBERCULAR FIXED DOSE COMBINATION 审中-公开
标题翻译：制备四种药物抗栓固定剂量组合的改进方法
公开(公告)号：WO2002087547A1
公开(公告)日：2002-11-07
申请号：PCT/IN2001/000093
申请日：2001-04-27
申请人： LUPIN LABORATORIES LIMITED , SEN, Himadri , JINDAL, Kour, Chand , DEO, Kishor, Dattatray , GANDHI, Krishnakant, Tulsiram
发明人： SEN, Himadri , JINDAL, Kour, Chand , DEO, Kishor, Dattatray , GANDHI, Krishnakant, Tulsiram
IPC分类号： A61K9/20
CPC分类号： A61K31/4409 , A61K9/2077 , A61K31/133 , A61K31/495 , A61K31/4965 , A61K2300/00
摘要： An improved process for preparation of a composition comprising fixed dose combination (FDC) of four anti-tubercular drugs viz. rifampicin, isoniazid, pyrazinamide and ethambutol hydrochloride, which improves the dissolution of poorly soluble drug rifampicin and hence improve its bioavailability. It further provides an improved process for preparation of a composition comprising fixed dose combination (FDC) of four anti-tubercular drugs viz. rifampicin, isoniazid, pyrazinamide and ethambutol hydrochloride, which improves the dissolution of poorly soluble drug rifampicin and hence improve its bioavailability, without use of a surfactant.
摘要翻译：用于制备包含四种抗结核药物的固定剂量组合（FDC）的组合物的改进方法，利福平，异烟肼，吡嗪酰胺和盐酸乙胺丁醇，改善了难溶性药物利福平的溶解，提高了其生物利用度。它还提供了一种改进的制备包含四种抗结核药物的固定剂量组合（FDC）的组合物的方法，利福平，异烟肼，吡嗪酰胺和盐酸乙胺丁醇，其改善了难溶性药物利福平的溶解，因此提高了其生物利用度，而不使用表面活性剂。

3. 发明申请

WO2002088149A2 A PROCESS FOR MANUFACTURE OF FOSINOPRIL SODIUM 审中-公开
标题翻译：一种制造FOSINOPRIL SODIUM的方法
公开(公告)号：WO2002088149A2
公开(公告)日：2002-11-07
申请号：PCT/IN2001/000144
申请日：2001-08-17
申请人： LUPIN LABORATORIES LIMITED , DUBEY, Sushil, Kumar , LAHIRI, Saswata , SINGH, Anil, Vir
发明人： DUBEY, Sushil, Kumar , LAHIRI, Saswata , SINGH, Anil, Vir
IPC分类号： C07F9/00
CPC分类号： C07F9/5721
摘要： The present invention discloses a process for the synthesis of fosinopril as a single desired isomer of high purity in two steps comprising of (a) preparation of fosinopril as a mixture of four diastereomers and (b) separation of the desired isomer from the mixture through formation of alkali metal salts followed by crystallisation.
摘要翻译：本发明公开了一种在两个步骤中合成作为高纯度的单一所需异构体的福辛普利的方法，包括（a）以四种非对映异构体的混合物制备福辛普利，和（b）通过形成从所述混合物中分离所需的异构体的碱金属盐，随后结晶。

4. 发明申请

WO2003010170A1 AN IMPROVED METHOD FOR PREPARATION OF CEFUROXIME AXETIL 审中-公开
标题翻译：一种改进的CEFUROXIME AXETIL的制备方法
公开(公告)号：WO2003010170A1
公开(公告)日：2003-02-06
申请号：PCT/IN2001/000134
申请日：2001-07-25
申请人： LUPIN LABORATORIES LIMITED , KANSAL, Vinod, Kumar , BHAT, Sunil, Gurudatt , MARUTIKUMAR, Tanguturi, Venkata , CHAVAN, Yuvaraj, Atmaram
发明人： KANSAL, Vinod, Kumar , BHAT, Sunil, Gurudatt , MARUTIKUMAR, Tanguturi, Venkata , CHAVAN, Yuvaraj, Atmaram
IPC分类号： C07D501/04
CPC分类号： C07D501/00
摘要： An improved method for synthesis of cefuroxime axetil of formula (I) in high purity substantially free of the corresponding 2-cephem(Δ 2 )-ester of formula (II) and other impurities. The compound produced is valuable as a prodrug ester of the corresponding cephalosporin- 4-carboxylic acid derivative i. e. cefuroxime, particularly suitable for oral administration in various animal species and in man for treatment of infections caused by gram-positive and gram-negative bacteria.
摘要翻译：用于合成基本上不含式（II）的相应2-头孢烯（DELTA 2））酯和其它杂质的高纯度的式（I）头孢呋辛酯的改进方法。所生产的化合物作为相应的头孢菌素-4-羧酸衍生物i的前药酯是有价值的。即头孢呋辛，特别适用于各种动物物种和人类口服给药，用于治疗由革兰氏阳性菌和革兰氏阴性细菌引起的感染。

5. 发明授权

EP1383779B1 A PROCESS FOR MANUFACTURE OF FOSINOPRIL SODIUM 有权
标题翻译：钠福辛普利的制备方法
公开(公告)号：EP1383779B1
公开(公告)日：2004-10-13
申请号：EP01967669.1
申请日：2001-08-17
申请人： LUPIN LABORATORIES LIMITED
发明人： DUBEY, Sushil, Kumar, Lupin Lab.Ltd. , LAHIRI, Saswata, Lupin Lab. Ltd. , SINGH, Anil, Vir, Lupin Lab. Ltd.
IPC分类号： C07F9/572
CPC分类号： C07F9/5721
摘要： The present invention discloses a process for the synthesis of fosinopril as a single desired isomer of high purity in two steps comprising of (a) preparation of fosinopril as a mixture of four diastereomers and (b) separation of the desired isomer from the mixture through formation of alkali metal salts followed by crystallisation.

6. 发明公开

EP1180032A2 USE OF NICORANDIL IN TREATMENT OF SEXUAL DYSFUNCTIONS OR FOR ENHANCEMENT OF SEXUAL FUNCTIONS 审中-公开
标题翻译：尼可地尔对阳痿治疗中的应用，提高SEXUELLLEN兴奋
公开(公告)号：EP1180032A2
公开(公告)日：2002-02-20
申请号：EP00939046.9
申请日：2000-04-28
申请人： Lupin Laboratories Limited
发明人： SAXENA, Ajit , BAKHLE, Dhananjay, Sadashiv,Lupin Lab. Limited
IPC分类号： A61K31/455 , A61P15/10
CPC分类号： A61K31/455 , Y10S514/906
摘要： The present invention discloses the use of nicorandil in treatment of male impotency and female sexual dysfunction. Nitric ester of N-(2-hydroxyethyl) nicotinamide or nicorandil, as it is better known is known as a drug for treatment of circulatory diseases. It is a pyridine derivative. Several clinical tests performed on male patients suffering from impotency including severe penile erectile dysfunction or female patients suffering from female sexual arousal dysfunction consistently showed excellent results. There was not a single instance of any of side effects or other symptoms of toxicity or deaths due to myocardial infarctions as was the case with other drugs including pyrazolopyrimidones compounds.

7. 发明公开

EP0659742A1 An improved method for the preparation of 2-chloro sulfinyl azetidin-4-one 失效
标题翻译： Verbidityes Verfahren zur Herstellung von 2-Chlorosulfinylazetidin-4-on。
公开(公告)号：EP0659742A1
公开(公告)日：1995-06-28
申请号：EP94309773.3
申请日：1994-12-23
申请人： LUPIN LABORATORIES LIMITED
发明人： Gupta, Niranjan Lal, Lupin Laboratories Limited , Sankaran, Ramanathan, Lupin Laboratories Limited , Sitabkhan, Sakina, Lupin Laboratories Limited
IPC分类号： C07D205/095 , C07D409/12 , C07D501/00
CPC分类号： C07D409/12 , C07D205/095 , C07D501/00 , Y02P20/55
摘要： An improved method for the preparation of 2-chloro sulfinyl azetidin-4-one of the general formula:

wherein R is hydrogen; C₁-C₃ alkyl; halomethyl; cyanomethyl; phenyl, substituted phenyl, phenoxy, benzyloxy or substituted benzyl with the substituent group selected from halo, alkyl, alkoxy, protected hydroxy, nitro, cyano and trifluoromethyl; a group of the formula R₂ -- O -- wherein R₂ is t-butyl, 2,2,2- trichloroethyl, benzyl or substituted benzyl; a group of the formula R₃-(O) n -CH₂ wherein R₃ is phenyl or substi-tuted phenyl with the substituent group selected from halo, alkyl, alkoxy, protected hydroxy, nitro, cyano or trifluoromethyl, 2-thienyl, 3-thienyl, 2-furyl, 3-furyl or 1,4-cyclohexadienyl, and n is 0 or 1; or a substituted aryl alkyl group of of formula

wherein R₄ has the same meaning as R₃ defined above and W is a protected hydroxy or protected amino group; and R₁ is a carboxylic acid protecting group selected from the group consisting of C₁-C₄ alkyl, 2,2,2-trihalo alkyl, benzyl, substituted benzyl, like p-nitrobenzyl, phenacyl, halo substituted phenacyl and benzhydryl, is disclosed. Such compound is prepared by reacting a penicillin sulfoxide ester of the general formula

wherein R and R₁ have the meanings defined above with an N-chloro halogenating agent in an inert organic solvent. The reaction is carried out in the presence of an acid scavening amount of a phosphate or hydrogen phosphate of an alkali metal, alkaline earth metal, ammonium, quaternary ammonium or mixtures of any thereof. These compounds find application as an intermediate in the production of cefaclor which are powerful anti-bacterial compounds.
摘要翻译：一种制备2-氯亚硫酰基氮杂环丁烷-4-酮的改进方法，其通式为：其中R为氢; C1-C3烷基; 卤; 氰; 苯基，取代的苯基，苯氧基，苄氧基或取代的苄基与选自卤素，烷基，烷氧基，保护的羟基，硝基，氰基和三氟甲基的取代基取代; 式R 2 -O - 的基团，其中R 2是叔丁基，2,2,2-三氯乙基，苄基或取代的苄基; 式R3-（O）n-CH2的基团，其中R3是苯基或具有选自卤素，烷基，烷氧基，保护的羟基，硝基，氰基或三氟甲基的取代基的苯基，2-噻吩基，3-噻吩基，2-呋喃基，3-呋喃基或1,4-环己二烯基，n为0或1; 或具有式CHEM的取代的芳基烷基，其中R 4具有与上述定义的R 3相同的含义，W是受保护的羟基或被保护的氨基; R1是选自C1-C4烷基，2,2,2-三卤代烷基，苄基，取代的苄基，如对硝基苄基，苯甲酰甲基，卤素取代的苯甲酰甲基和二苯甲基的羧酸保护基。通过使惰性有机溶剂中的具有上述定义的R和R 1具有N-氯卤化剂的通式的青霉素亚砜酯反应来制备该化合物。该反应在酸清除量的碱金属，碱土金属，铵，季铵的磷酸盐或磷酸氢盐或其混合物的存在下进行。这些化合物可用作生产头孢克洛的中间体，它们是强大的抗菌化合物。

8. 发明公开

EP1383779A2 A PROCESS FOR MANUFACTURE OF FOSINOPRIL SODIUM 有权
标题翻译：钠福辛普利的制备方法
公开(公告)号：EP1383779A2
公开(公告)日：2004-01-28
申请号：EP01967669.1
申请日：2001-08-17
申请人： LUPIN LABORATORIES LIMITED
发明人： DUBEY, Sushil, Kumar,Lupin Lab.Ltd. , LAHIRI, Saswata,Lupin Lab. Ltd. , SINGH, Anil, Vir,Lupin Lab. Ltd.
IPC分类号： C07F9/572
CPC分类号： C07F9/5721
摘要： The present invention discloses a process for the synthesis of fosinopril as a single desired isomer of high purity in two steps comprising of (a) preparation of fosinopril as a mixture of four diastereomers and (b) separation of the desired isomer from the mixture through formation of alkali metal salts followed by crystallisation.

9. 发明公开

EP0976751A1 A process for the isomerisation of an N-7 isomer into an N-9 isomer useful in the synthesis of acyclic nucleosides 失效
标题翻译：一种用于在N-9异构体的合适的N-7异构体的无环核苷的合成的异构化过程
公开(公告)号：EP0976751A1
公开(公告)日：2000-02-02
申请号：EP99116909.5
申请日：1996-04-09
申请人： LUPIN LABORATORIES LIMITED
发明人： Kumar, Ashoke, Lupin Laboratories Ltd. , Singh, Dharmendra, Lupin Laboratories Ltd. , Wani, Mukesh Jagannath, Lupin Laboratories Ltd. , Joshi, Narendra Sriram, Lupin Laboratories Ltd. , Thombre, Pravin Sahadev, Lupin Laboratories Ltd. , Rawat, Ajay Singh, Lupin Laboratories Ltd.
IPC分类号： C07D473/18
CPC分类号： C07D473/00
摘要： This invention relates to a process for the isomerisation of the N-7 isomer N 2 -acetyl-7-[(2-acetoxyethoxy)methyl] guanine into the N-9 isomer N 2 -acetyl-9-[(2-acetoxyethoxy)methyl] guanine, which is a useful intermediate in the synthesis of acyclic nucleosides.
摘要翻译：本发明涉及一种用于在N-7异构体N中的异构化<2>乙酰基7-A（2-乙酰氧基 - 乙氧基）methylÜ鸟嘌呤到N-9异构体Ñ<2>乙酰基9-A（2 -acetoxyethoxy）methylÜ鸟嘌呤，所有这是在无环核苷的合成中有用的中间体。

10. 发明公开

EP0866137A1 Process for producing calcium salt of (-)-Erythrohydroxycitric acid 失效
标题翻译： Verfahren zur Herstellung von Calcium（ - ） - 红细胞生成素
公开(公告)号：EP0866137A1
公开(公告)日：1998-09-23
申请号：EP97301777.5
申请日：1997-03-17
申请人： LUPIN LABORATORIES LIMITED
发明人： Sharma, Nina, Lupin Lab. Ltd. Nat. Pro. Div. , Parashuraman, Meena, Lupin Lab. Ltd. Nat. Pro.Div. , Raman, Girija, Lupin Lab. Ltd. Nat. Pro. Div.
IPC分类号： C12S3/00 , C07C59/245
CPC分类号： C12P7/48 , C07C59/245
摘要： A process for extraction of hydroxycitric acid as calcium salt from the fruit rind of Garcinia species such as Garcinia cambogia , Garcinia indica and Garcinia atroviridis , which comprises reaction of an aqueous suspension of Garcinia rind with a mixture of pectic enzymes such as polygalactouronase (PG) and pectin lysase (PL), at a temperature of 40°C followed by addition of an alkali such as sodium hydroxide and, from the intermediate alkali metal salt of hydroxycitric acid the corresponding calcium salt is prepared by addition of calcium chloride. The calcium salt of (-)-hydroxycitric acid is therapeutically active component.
摘要翻译：从藤黄属（Garcinia cambogia），藤黄（Garcinia indica）和藤黄属（Garcinia atroviridis）的果皮中提取羟基柠檬酸作为钙盐的方法，其包括藤黄的水性悬浮液与果胶酶的混合物如聚半乳糖醛酸酶（PG）和果胶裂解酶（PL），在40℃的温度下加入碱如氢氧化钠，从羟基柠檬酸的中间体碱金属盐中加入氯化钙制备相应的钙盐。（ - ） - 羟基柠檬酸钙盐是治疗活性成分。

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