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51. 发明申请

WO2007129328A2 PROCESS FOR PREPARING 2-[PYRIDINYL]SULFINYL-SUBSTITUTED BENZIMIDAZOLES 审中-公开
标题翻译：制备2- [吡啶基]磺酰基取代苯并咪唑的方法
公开(公告)号：WO2007129328A2
公开(公告)日：2007-11-15
申请号：PCT/IN2007/000158
申请日：2007-04-23
申请人： CADILA HEALTHCARE LIMITED , SHAH, Niraj, Shyamlal , DWIVEDI, Shriprakash, Dhar
发明人： SHAH, Niraj, Shyamlal , DWIVEDI, Shriprakash, Dhar
CPC分类号： C07D401/12
摘要： A process for the preparation of 2-[(pyridinyl)methyl]sulfinyl-benzimidazole of Formula (I) or a pharmaceutically acceptable salt, hydrate, or solvate thereof, wherein R 1 is selected from the group consisting of hydrogen or substituted or unsubstituted C 1 -C 4 alkoxy; R 2 and R 4 are independently selected from the group consisting of hydrogen, C 1 -C 4 alkyl or C 1 -C 4 alkoxy; R 3 is selected from the group consisting of substituted or unsubstituted C 1 -C 4 alkoxy is disclosed. The process comprises oxidizing thioether compound of formula (II) in absence of base, wherein R 1 , R 2 , R 3 and R 4 is same as described above, with N-halosuccinimide in presence of water, optionally converting into a pharmaceutically acceptable salt, hydrate, or solvate thereof.
摘要翻译：制备式（I）的2 - [（吡啶基）甲基]亚磺酰基 - 苯并咪唑或其药学上可接受的盐，水合物或溶剂化物的方法，其中R 1选自的氢或取代或未取代的C 1 -C 4烷氧基; R 2和R 4独立地选自氢，C 1 -C 4烷基或C 1 -C 4烷基， ç_{1 -C _{4 烷氧基; R 3 3选自取代或未取代的C 1 -C 4烷氧基。该方法包括在不存在碱的情况下氧化式（II）的硫醚化合物，其中R 1，R 2，R 3和R 3 > 4 与上述相同，N-卤代琥珀酰亚胺在水存在下，任选转化成其药学上可接受的盐，水合物或溶剂化物。}}

52. 发明申请

WO2007096753A3 PROCESS FOR PREPARING HIGHLY PURE SIMVASTATIN 审中-公开
公开(公告)号：WO2007096753A3
公开(公告)日：2007-08-30
申请号：PCT/IB2007/000429
申请日：2007-02-21
申请人： CADILA HEALTHCARE LIMITED , UPADHYAY, G., Umesh , SHAH, Niraj, Kumar, Shyamial , KUMAR, Rajiv , DWIVEDI, Shri, Prakash, Dhar
发明人： UPADHYAY, G., Umesh , SHAH, Niraj, Kumar, Shyamial , KUMAR, Rajiv , DWIVEDI, Shri, Prakash, Dhar
IPC分类号： C07D309/30 , A61K31/351 , C07F7/18 , A61P3/06
摘要： The present invention discloses a solid compound of silylated simvastatin having formula (I). Said compound of Formula (I) is prepared by hydrolyzing lovastatin to diol lactone; converting said diol lactone to silylated lactone; and acylating said silylated lactone to produce silylated simvastatin.

53. 发明申请

WO2007096751A1 PROCESS FOR THE PREPARATION OF ATORVASTATIN CALCIUM 审中-公开
标题翻译：制备ATORVASTATIN钙的方法
公开(公告)号：WO2007096751A1
公开(公告)日：2007-08-30
申请号：PCT/IB2007/000426
申请日：2007-02-21
申请人： CADILA HEALTHCARE LIMITED , PATEL, Dhimant, Jasubhai , KUMAR, Rajiv , DWIVEDI, Shri Prakash Dhar
发明人： PATEL, Dhimant, Jasubhai , KUMAR, Rajiv , DWIVEDI, Shri Prakash Dhar
IPC分类号： C07D405/06 , A61K31/4015
CPC分类号： C07D405/06
摘要： The present invention relates to process for the preparation of atorvastatin calcium. The process provides the novel approach for the synthesis of an important intermediate atorvastatin protected diol chemically (4R-cis)-6-[-2-[3-phenyl-4-(phenyl- carbamoyl)-2-(4-flourophenyl)-5-(1-methyl-ethyl)-pyrrol-1-yl]-ethyl]-2,2-dimethyl- [1,3]dioxane-4-yl-acetic acid-tertriay butyl ester for atorvastatin calcium i.e. [R- (R*,R*)]-2-(4-fluorophenyl-β,δ-dihydroxy-5-(1-methylethyl)-3-phenyl-4- [(phenylamino) carbonyl]-1H-pyrrole-1-heptanoic acid calcium salt (2:1). The present invention relates the use of amino side chain i.e [6-(2-aminoethyl)-2,2,-dimethyl- [1,3]dioxan-4-yl]-acetic acid tert-butyl ester and stetter compound i.e. 4-(4- Fluoroρhenyl)-2-isobutryl-4-oxo-N-phenyl butryl amide as an important starting materials for the preparation of atorvastatin protected diol in the high yield and thereby the recovery of amino side chain with an industrially applicable process.
摘要翻译：本发明涉及制备阿托伐他汀钙的方法。该方法提供了用于合成重要的中间体阿托伐他汀保护的二醇（4R-顺式）-6 - [ - 2- [3-苯基-4-（苯基 - 氨基甲酰基）-2-（4-氟苯基） - 5-（1-甲基 - 乙基） - 吡咯-1-基] - 乙基] -2,2-二甲基 - [1,3]二恶烷-4-基 - 乙酸 - 叔丁基酯，用于阿托伐他汀钙，即[R- （R *，R *）] - 2-（4-氟苯基-β，d-二羟基-5-（1-甲基乙基）-3-苯基-4 - [（苯基氨基）羰基] -1H-吡咯-1-庚酸本发明涉及氨基侧链，即[6-（2-氨基乙基）-2,2'-二甲基 - [1,3]二烷-4-基] - 乙酸叔丁酯和酯化合物，即4-（4-氟苯乙基）-2-异丁基-4-氧代-N-苯基丁酰胺，作为以高产率制备阿托伐他汀保护的二醇的重要起始原料，从而用工业上适用的方法回收氨基侧链。

54. 发明申请

WO2005085199A1 NOVEL POLYMORPHS OF ETORICOXIB 审中-公开
标题翻译： ETORICOXIB的新型POLYMORPHS
公开(公告)号：WO2005085199A1
公开(公告)日：2005-09-15
申请号：PCT/IN2005/000009
申请日：2005-01-07
申请人： CADILA HEALTHCARE LIMITED , LOHRAY, Braj, Bhushan , LOHRAY, Vidya, Bhushan , DAVE, Mayank, Ghanshyambhai
发明人： LOHRAY, Braj, Bhushan , LOHRAY, Vidya, Bhushan , DAVE, Mayank, Ghanshyambhai
IPC分类号： C07D213/22
CPC分类号： C07D213/22
摘要： The present invention provides new crystalline forms of Etoricoxib of formula I or mixture thereof. Another objective of the present invention is to provide a process for the preparation of novel forms of Etoricoxib or mixture thereof. Yet another objective is to provide novel crystalline forms or mixture of Etoricoxib which are stable. Yet anothr objective is to provide a process for the preparation of pharmaceutical composition comprising the said novel forms of Etoricoxib. An an embodiment of the present invention pharmaceutical compositions containing one or more of the new forms described in the present invention is provided. A further objective of the present invention is to provide uses of the novel forms of Etoricoxib for the treatment of COX-2 mediated disorders in a mammal including human.
摘要翻译：本发明提供了式I的Etoricoxib或其混合物的新结晶形式。本发明的另一个目的是提供一种制备新型形式的埃托替尼或其混合物的方法。另一个目标是提供稳定的新型结晶形式或Etoricoxib的混合物。然而，另一个目的是提供一种制备包含所述新型形式的埃托替尼的药物组合物的方法。本发明的一个实施方案提供了包含本发明中所述的一种或多种新形式的药物组合物。本发明的另一个目的是提供新型形式的Etoricoxib用于治疗哺乳动物包括人的COX-2介导的病症的用途。

55. 发明申请

WO2005068464A2 PROCESS FOR PREPARING TADALAFIL AND ITS INTERMEDIATES 审中-公开
标题翻译：制备TADALAFIL及其中间体的方法
公开(公告)号：WO2005068464A2
公开(公告)日：2005-07-28
申请号：PCT/IN2004/000389
申请日：2004-12-14
申请人： CADILA HEALTHCARE LIMITED , LOHRAY, Braj, Bhushan , LOHRAY, Vidya, Bhushan , PATEL, Sunil, Indulal
发明人： LOHRAY, Braj, Bhushan , LOHRAY, Vidya, Bhushan , PATEL, Sunil, Indulal
IPC分类号： C07D471/14
CPC分类号： C07D471/04 , C07D471/14
摘要： The present invention relates to two novel forms of Tadalafil which differ in their bulk densities. The invention also relates to an improved process for the preparation of Tadalafil and its intermediates.
摘要翻译：本发明涉及两种不同体积密度的他达拉非的新型形式。本发明还涉及一种改进的他达拉非及其中间体的制备方法。

56. 发明申请

WO2004081016A1 POLYMORPHS AND AMORPHOUS FORM OF (S) - (+) -CLOPIDOGREL BISULFATE 审中-公开
标题翻译：（S） - （+） - 乳酸双歧杆菌的多聚体和非晶形式
公开(公告)号：WO2004081016A1
公开(公告)日：2004-09-23
申请号：PCT/IN2003/000053
申请日：2003-03-12
申请人： CADILA HEALTHCARE LIMITED , LOHRAY, Braj, Bhushan , LOHRAY, Vidya, Bhushan , PANDEY, Bipin , DAVE, Mayank, Ghanshyambhai
发明人： LOHRAY, Braj, Bhushan , LOHRAY, Vidya, Bhushan , PANDEY, Bipin , DAVE, Mayank, Ghanshyambhai
IPC分类号： C07D495/04
CPC分类号： C07D495/04
摘要： The present invention relates to new polymorphs of S-(+)-Clopidogrel bisulfate and a process for preparing the same.
摘要翻译：本发明涉及S - （+） - 氯吡格雷硫酸氢盐的新型多晶型物及其制备方法。

57. 发明申请

WO2004002445A2 NOVEL FLOATING DOSAGE FORM 审中-公开
标题翻译：新的浮动剂型
公开(公告)号：WO2004002445A2
公开(公告)日：2004-01-08
申请号：PCT/IN2003/000229
申请日：2003-06-25
申请人： CADILA HEALTHCARE LIMITED , LOHRAY, Braj, Bhushan , TIWARI, Sandip, B. , PAI, Raveendra, M. , MURTHY, Krishna, T. , MEHTA, Pavak, R.
发明人： LOHRAY, Braj, Bhushan , TIWARI, Sandip, B. , PAI, Raveendra, M. , MURTHY, Krishna, T. , MEHTA, Pavak, R.
IPC分类号： A61K9/00
CPC分类号： A61K9/0065
摘要： Present invention relates to a novel pharmaceutical composition containing an active ingredient(s) which is retained in the stomach or upper part of gastrointestinal tract for controlled delivery of medicament for improved local treatment, and/or better absorption from upper parts of gastrointestinal tract for effective therapeutic results. Present invention also provides a method for preparation of the said dosage form preferably in the form of a bilayer tablet, in which one layer constitutes for spatial control and the other being for temporal control.
摘要翻译：本发明涉及含有活性成分的新型药物组合物，其保留在胃或胃肠道上部，用于控制递送用于改善局部治疗的药物和/或从胃肠道上部更好地吸收以有效地治疗结果。本发明还提供了优选以双层片剂形式制备所述剂型的方法，其中一层构成用于空间控制，另一层构成用于时间控制。

58. 发明申请

WO2003082864A3 ANTIINFECTVE COMPOUNDS, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 审中-公开
公开(公告)号：WO2003082864A3
公开(公告)日：2003-10-09
申请号：PCT/IN2003/000081
申请日：2003-03-26
申请人： CADILA HEALTHCARE LIMITED , LOHRAY, Braj, Bhushan , LOHRAY, Vidya, Bhushan , SRIVASTAVA, Brijesh, Kumar
发明人： LOHRAY, Braj, Bhushan , LOHRAY, Vidya, Bhushan , SRIVASTAVA, Brijesh, Kumar
IPC分类号： C07D413/12
摘要： The present invention relates to novel compounds of general formula (I), their analogs, their derivatives, their stereoisomers, tautomeric forms, novel intermediates involved in their synthesis, their pharmaceutically acceptable salts and pharmaceutical compositions containing them. The present invention also relates to a process of preparing compounds of general formula (I), their analogs, their derivatives, their stereoisomers, their tautomeric forms, their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, pharmaceutical compositions containing them, and novel intermediates (I) involved in their synthesis. The compound of the present invention is useful in the treatment of a number of human and veterinary pathogens, including aerobic as well as anaerobic Gram-positive and Gram-negative organisms.

59. 发明申请

WO2021234655A2 FC VARIANT AND PREPARATION THEREOF 审中-公开
公开(公告)号：WO2021234655A2
公开(公告)日：2021-11-25
申请号：PCT/IB2021/054423
申请日：2021-05-21
申请人： CADILA HEALTHCARE LIMITED
发明人： MENDIRATTA, Sanjeev Kumar , KASERA, Ramkrashan , SINGH, Arun Kumar , PARIKH, Aashini , KALITA, Pankaj , HANDA, Satish , SHAH, Anushree , PATEL, Heena , PANDYA, Hardik , SHARMA, Vibhuti , PATEL, Chirag , SONI, Swagat , VYAS, Narayani
IPC分类号： C07K16/00 , A61K39/00 , A61K2039/505 , C07K2317/52 , C07K2317/524 , C07K2317/526 , C07K2317/70 , C07K2317/732 , C07K2317/92 , C07K2319/30
摘要： The present invention relates to Fc variant protein and preparation thereof. Said Fc variant has altered binding affinity towards FcRn. Fc variant prepared according to the current invention can be used for making FcRn antagonist composition or can be used for making an Fc variant containing drug or molecule with altered effector function.

60. 发明申请

WO2021214703A1 A VACCINE AGAINST SARS-COV-2 AND PREPARATION THEREOF 审中-公开
公开(公告)号：WO2021214703A1
公开(公告)日：2021-10-28
申请号：PCT/IB2021/053321
申请日：2021-04-22
申请人： CADILA HEALTHCARE LIMITED
发明人： PATEL, Pankaj
IPC分类号： A61K39/215
摘要： The current invention provides a DNA construct comprising S gene or S1 gene region of 2019-nCoV spike-S protein. The DNA construct of the present invention comprises DNA plasmid vector carrying S gene or S1 gene region of 2019-nCoV spike-S protein. The vector may further comprise a gene encoding IgE signal peptide or a gene encoding t-PA signal peptide. The DNA construct according to the present invention is further used in the preparation of an immunogenic composition or a vaccine for treating or preventing corona virus or its related diseases.

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