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1. 发明授权

US5608061A Process for preparing 1,4,8,11-tetraazacyclotetradecane 失效
标题翻译：制备1,4,8,11-四氮杂环十四烷的方法
公开(公告)号：US5608061A
公开(公告)日：1997-03-04
申请号：US510207
申请日：1995-08-02
申请人： Lech Ciszewski , John Amedio , Prasad Kapa , Andrew Kucerovy , George T. Lee
发明人： Lech Ciszewski , John Amedio , Prasad Kapa , Andrew Kucerovy , George T. Lee
IPC分类号： C07D257/02 , C07D255/02
CPC分类号： C07D257/02
摘要： An improved process for preparing 1,4,8,11-tetraazacyclotetradecane comprising the tetratosylation of an acyclic tetraamine to obtain a tetratoluenesulfonamide compound in a first step, the cyclization of said sulfonamide compound to obtain tetratosyl cyclam in a second step, and the detosylation of tetratosyl cyclam in a third step followed by basification to obtain the desired 1,4,8,11-tetraazacyclotetradecane.
摘要翻译：一种制备1,4,8,11-四氮杂环十四烷的改进方法，其包括无环四胺的四甲硅烷基化以在第一步中获得四磺酰胺化合物，在第二步中环化所述磺酰胺化合物以获得四基体环已烷，并进行脱甲苯基化在第三步骤中进行四糖基环化，然后碱化以获得所需的1,4,8,11-四氮杂环十四烷。

2. 发明授权

US5691304A Improved process for preparing polymyxin B/dextran conjugates 失效
标题翻译：制备多粘菌素B /葡聚糖共轭物的改进方法
公开(公告)号：US5691304A
公开(公告)日：1997-11-25
申请号：US449436
申请日：1995-05-25
申请人： Prasad Kapa , Gleb Kardash , Andrew Kucerovy , Philip Lake , Paul G. Mattner , Russell C. Petter , Mahavir Prashad , Sushil Sharma
发明人： Prasad Kapa , Gleb Kardash , Andrew Kucerovy , Philip Lake , Paul G. Mattner , Russell C. Petter , Mahavir Prashad , Sushil Sharma
IPC分类号： A61K38/08 , A61K47/48 , A61P31/04 , A61K38/10 , C07K5/00
CPC分类号： A61K47/4823
摘要： An improved process for producing a water-soluble polymyxin B/dextran conjugate comprises the step of reacting polymyxin B or pharmaceutically acceptable salt thereof with dextran in an aqueous media at a pH of about 9.3 to 10.
摘要翻译：制备水溶性多粘菌素B /葡聚糖结合物的改进方法包括在约9.3至10的pH下，使多粘菌素B或其药学上可接受的盐与葡聚糖在水性介质中反应的步骤。

3. 发明申请

US20060035941A1 Calcium salts of indole derived statins 审中-公开
标题翻译：吲哚衍生的他汀类钙盐
公开(公告)号：US20060035941A1
公开(公告)日：2006-02-16
申请号：US10517874
申请日：2003-06-12
申请人： Guang-Pei Chen , Prasad Kapa , Paul Sutton
发明人： Guang-Pei Chen , Prasad Kapa , Paul Sutton
IPC分类号： A61K31/404 , C07D209/04
CPC分类号： C07D209/24
摘要： The present invention provides calcium salts of indole derived statins of the formula (IA) wherein R1, is alkyl, cycloalkyl or aralkyl; R2, R3 and R4 are independently hydrogen, halogen or alkyl; R5 and R6 are independently hydrogen, halogen, alkyl, cycloalkyl, aralkyl, alkoxy or aralkoxy; and the hydroxyl group at the 3position is in the R-configuration and at the 5position in the S-configuration; or an enantiomer thereof; or a hydrate thereof; as obtainable by the methods of the present invention. More specifically, the invention provides a calcium salt of formula (IA) wherein R1, is isopropyl, R2 is fluorine and R3, R4, R5 and R6 are hydrogen, designated herein as Fluvastatin calcium, in a highly crystalline form. Furthermore, the present invention is directed to methods for the preparation of the crystalline Fluvastatin calcium, and to pharmaceutical compositions comprising the crystalline form.
摘要翻译：本发明提供式（IA）的吲哚衍生的他汀类的钙盐，其中R 1是烷基，环烷基或芳烷基; R 2，R 3和R 4独立地是氢，卤素或烷基; R 5和R 6独立地是氢，卤素，烷基，环烷基，芳烷基，烷氧基或芳烷氧基; 并且3位上的羟基处于R-构型，在5-构型中为5位; 或其对映体; 或其水合物; 如通过本发明的方法可获得的。更具体地，本发明提供式（IA）的钙盐，其中R 1是异丙基，R 2是氟和R 3， R 4，R 5和R 6是高度结晶形式的本文称为氟伐他汀钙的氢。此外，本发明涉及制备结晶氟伐他汀钙的方法以及包含结晶形式的药物组合物。

4. 发明申请

US20150232446A1 MANUFACTURING PROCESS FOR PYRIMIDINE DERIVATIVES 有权
标题翻译：吡啶衍生物的制备方法
公开(公告)号：US20150232446A1
公开(公告)日：2015-08-20
申请号：US14705013
申请日：2015-05-06
申请人： John Vincent Calienni , Dietmar Flubacher , Baoqing Gong , Prasad Kapa , Hui Liu , Pascal Michel , Rasmus Mose , Maria Caterina Testa
发明人： John Vincent Calienni , Dietmar Flubacher , Baoqing Gong , Prasad Kapa , Hui Liu , Pascal Michel , Rasmus Mose , Maria Caterina Testa
IPC分类号： C07D401/04 , C07D213/72 , C07F5/02
CPC分类号： C07D401/04 , A61K31/535 , C07D213/72 , C07D413/14 , C07F5/025 , C07F5/04
摘要： The invention relates to processes for manufacturing a compound of formula 5, or a stereoisomer, tautomer or a salt thereof, wherein the substituents are as defined in the specification. The invention further relates to new manufacturing processes for specific solid forms of Compound A and its salts, to such solid forms and to use of such solid forms for the therapeutic treatment of warm-blooded animals.
摘要翻译：本发明涉及制备式5化合物或其立体异构体，互变异构体或其盐的方法，其中取代基如说明书中所定义。本发明还涉及用于化合物A及其盐的特定固体形式的这种固体形式的新制备方法，以及这些固体形式用于治疗温血动物的新方法。

5. 发明申请

US20070179298A1 Chemical process for the preparation of intermediates to obtain n-formyl hydroxy-lamine compounds 失效
标题翻译：用于制备中间体以获得正甲酰基羟基 - 胺化合物的化学方法
公开(公告)号：US20070179298A1
公开(公告)日：2007-08-02
申请号：US10544919
申请日：2004-02-20
申请人： Mahavir Prashad , Hong-Yong Kim , Bin Hu , Joel Slade , Prasad Kapa , Michael Girgis
发明人： Mahavir Prashad , Hong-Yong Kim , Bin Hu , Joel Slade , Prasad Kapa , Michael Girgis
IPC分类号： A61K31/4439 , C07D417/02 , C07D403/02
CPC分类号： C07D401/12 , C07B2200/07 , C07C51/487 , C07C239/20 , C07C59/01
摘要： Improved processes for preparing intermediates useful for preparing antibacterial N-[1-oxo-2-alkyl-3-(N-hydroxyformamido)-propyl}-(carbonylamino-aryl or -heteroaryl)-azacyclo4-7alkanes or thiazacyclo4-7alkanes, which have one or more of the following features: (1) make use of a particular β-lactam intermediate; (2) which make use of a particular resolving agents, enantiomerically pure substituted propionic acids, especially (R)-2-butyl-3-hydroxy-propionic acid; (3) which avoid the use of hydrogen peroxide; and (4) which facilitate selective debenzylation reducing production of waste by-products.
摘要翻译：用于制备可用于制备抗菌N- [1-氧代-2-烷基-3-（N-羟基甲酰氨基） - 丙基} - （羰基氨基 - 芳基或 - 杂芳基） - 偶氮基-4-7烷烃或噻唑烷-4-醇的中间体的改进方法，其具有一个或多个以下特征：（1）利用特定的β-内酰胺中间体; （2），其使用特定的拆分剂，对映体纯的取代的丙酸，特别是（R）-2-丁基-3-羟基 - 丙酸; （3）避免使用过氧化氢; 和（4）促进选择性脱苄基化减少废弃副产物的生产。

6. 发明申请

US20070135502A1 HETEROCYCLIC COMPOUNDS AND METHODS OF USE 审中-公开
标题翻译：杂环化合物和使用方法
公开(公告)号：US20070135502A1
公开(公告)日：2007-06-14
申请号：US11619936
申请日：2007-01-04
申请人： Andrew Bach , Prasad Kapa , George Lee , Eric Loeser , Michael Sabio , James Stanton , Thalaththani Vedananda
发明人： Andrew Bach , Prasad Kapa , George Lee , Eric Loeser , Michael Sabio , James Stanton , Thalaththani Vedananda
IPC分类号： A61K31/42 , A61K31/404 , A61K31/4025 , A61K31/401 , C07D413/02 , C07D411/02
CPC分类号： C07D205/04 , C07D207/16 , C07D209/42 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12
摘要： Compounds of the formula provide pharmacological agents which are potent agonists of Peroxisome Proliferator-Activated Receptors (PPARs). Accordingly, the compounds of the instant invention are useful for the treatment of conditions mediated by the PPAR receptor activity in mammals. Such conditions include dyslipidemia, hyperlipidemia, hypercholesteremia, atherosclerosis, hypertriglyceridemia, heart failure, myocardial infarction, vascular diseases, cardiovascular diseases, hypertension, obesity, inflammation, arthritis, cancer, Alzheimer's disease, skin disorders, respiratory diseases, ophthalmic disorders, inflammatory bowel diseases, ulcerative colitis and Crohn's disease. The compounds of the present invention are particularly useful in mammals as hypoglycemic agents for the treatment and prevention of conditions in which impaired glucose tolerance, hyperglycemia and insulin resistance are implicated, such as type-1 and type-2 diabetes, and Syndrome X. Preferred are the compounds of the invention which are dual agonists of PPARα and PPARγ receptors.
摘要翻译：配方的化合物提供作为过氧化物酶体增殖物激活受体（PPARs）的有效激动剂的药理学试剂。因此，本发明的化合物可用于治疗由哺乳动物中的PPAR受体活性介导的病症。这些病症包括血脂异常，高脂血症，高胆固醇血症，动脉粥样硬化，高甘油三酯血症，心力衰竭，心肌梗死，血管疾病，心血管疾病，高血压，肥胖症，炎症，关节炎，癌症，阿尔茨海默病，皮肤病，呼吸系统疾病，眼科疾病，炎症性肠病，溃疡性结肠炎和克罗恩病。本发明的化合物在哺乳动物中特别可用作降血糖药，用于治疗和预防葡萄糖耐量降低，高血糖症和胰岛素抵抗等疾病，如1型和2型糖尿病，以及X综合征。是本发明的化合物，它们是PPARα和PPARγ受体的双重激动剂。

7. 发明授权

US5811544A Process for preparing 1,4,8,11-tetraazacyclotetradecane 失效
标题翻译：制备1,4,8,11-四氮杂环十四烷的方法
公开(公告)号：US5811544A
公开(公告)日：1998-09-22
申请号：US690105
申请日：1996-07-30
申请人： Orin Tempkin , Prasad Kapa
发明人： Orin Tempkin , Prasad Kapa
IPC分类号： C07D257/02 , C07D255/02
CPC分类号： C07D257/02
摘要： An improved process for preparing 1,4,8,11-tetraazacyclotetradecane comprising the bisacylation of an acyclic diamine to obtain a dichlorodiamide compound in a first step, the cyclization of said diamide compound to obtain dioxocyclam in a second step, and the reduction of dioxocyclam in a third step to obtain the desired 1,4,8,11-tetraazacyclotetradecane.
摘要翻译：一种改进的制备1,4,8,11-四氮杂环十四烷的方法，其包括在第一步中无环二胺的双酰化得到二氯二酰胺化合物，第二步中所述二酰胺化合物环化以获得二氧杂环，并且还原二氧环在第三步中获得所需的1,4,8,11-四氮杂环十四烷。

8. 发明授权

US5612478A Process for preparing 1,1'-[1,4-phenylenebis-(methylene)]-bis-1,4,8,11-tetraazacyclotetradecan e 失效
标题翻译：制备1,1' - [1,4-亚苯基双（亚甲基）] - 双-1,4,8,11-四氮杂环十四烷的方法
公开(公告)号：US5612478A
公开(公告)日：1997-03-18
申请号：US413582
申请日：1995-03-30
申请人： David Xu , Prasad Kapa , Oljan Repic , Thomas J. Blacklock
发明人： David Xu , Prasad Kapa , Oljan Repic , Thomas J. Blacklock
IPC分类号： C07C233/00 , C07C233/36 , C07C303/00 , C07C311/18 , C07D257/02
CPC分类号： C07C233/36 , C07C311/18 , C07D257/02
摘要： An improved process for preparing 1,1'-[1,4-phenylenebis-(methylene)]-bis-1,4,8,11-tetraazacyclotetradecane comprising the selective functionalization of an acyclic tetraamine, and subsequent dimerization and hydrolyzation/tosylation to obtain a 1,4-phenylenebis-methylene bridged hexatosyl acyclic precursor in a first step, the cyclization of said precursor to obtain a hexatosyl cyclam dimer in a second step, and the detosylation of said cyclam dimer in a third step followed by basification to obtain the desired 1,1'-[1,4-phenylenebis-(methylene)]-bis-1,4,8,11-tetraazacyclotetradecane.
摘要翻译：制备1,1' - [1,4-亚苯基双（亚甲基）] - 双-1,4,8,11-四氮杂环十四烷的改进方法，其包括无环四胺的选择性官能化，随后二聚和水解/甲苯磺酰化至在第一步中获得1,4-亚苯基双 - 亚甲基桥联的六碳酰基非环状前体，在第二步中环化所述前体以获得己糖基环胞二聚体，并在第三步中对所述环化二聚体进行脱甲苯基化，然后碱化得到所需的1,1' - [1,4-亚苯基双（亚甲基）] - 双-1,4,8,11-四氮杂环十四烷。

9. 发明授权

US5606053A Process for preparing 1,1'-[1,4-phenylenebis-(methylene)]-bis-1,4,8,11-tetraazacyclotetradecan e 失效
标题翻译：制备1,1' - [1,4-亚苯基双（亚甲基）] - 双-1,4,8,11-四氮杂环十四烷的方法
公开(公告)号：US5606053A
公开(公告)日：1997-02-25
申请号：US434142
申请日：1995-05-02
申请人： Mahavir Prashad , Prasad Kapa
发明人： Mahavir Prashad , Prasad Kapa
IPC分类号： C07C311/18 , C07D257/02 , C07D255/00 , C07D255/02
CPC分类号： C07C311/18 , C07D257/02
摘要： An improved process for preparing 1,1'-[1,4-phenylenebis-(methylene)]-bis-1,4,8,11-tetraazacyclotetradecane comprising the selective functionalization of an acyclic tetraamine to obtain an acyclic ditosyl intermediate and an acyclic tritosyl intermediate in a first step, the independent dimerization/tosylation of the ditosyl intermediate and dimerization of the tritosyl intermediate to obtain a 1,4-phenylenebis-methylene bridged hexatosyl acyclic precursor in a second step, the cyclization of said precursor to obtain a hexatosyl cyclam dimer in a third step, and the detosylation of said cyclam dimer in a fourth step followed by basification to obtain the desired 1,1'-[1,4-phenylenebis-(methylene)]-bis-1,4,8,11-tetraazacyclotetradecane.
摘要翻译：制备1,1' - [1,4-亚苯基双（亚甲基）] - 双-1,4,8,11-四氮杂环十四烷的改进方法，其包括无环四胺的选择性官能化以获得无环二硫代基中间体和非环状在第一步中的三羟甲基中间体，二硫代基中间体的独立二聚化/甲苯磺酰化和三乙基中间体的二聚作用，以在第二步中获得1,4-亚苯基双 - 亚甲基桥连的六碳酰基非环状前体，所述前体环化以获得六第三步中的环酰胺二聚体和第四步骤中所述环酰二聚体的去甲苯基化，接着进行碱化，得到所需的1,1' - [1,4-亚苯基双（亚甲基）] - 双-1,4,8， 11-四氮杂环十四烷。

10. 发明授权

US09359326B2 Manufacturing process for pyrimidine derivatives 有权
标题翻译：嘧啶衍生物的制备方法
公开(公告)号：US09359326B2
公开(公告)日：2016-06-07
申请号：US14705013
申请日：2015-05-06
申请人： John Vincent Calienni , Baoqing Gong , Prasad Kapa , Hui Liu
发明人： John Vincent Calienni , Baoqing Gong , Prasad Kapa , Hui Liu
IPC分类号： C07D401/04 , C07D213/72 , C07F5/02
CPC分类号： C07D401/04 , A61K31/535 , C07D213/72 , C07D413/14 , C07F5/025 , C07F5/04
摘要： The invention relates to processes for manufacturing a compound of formula 5, or a stereoisomer, tautomer or a salt thereof, wherein the substituents are as defined in the specification. The invention further relates to new manufacturing processes for specific solid forms of Compound A and its salts, to such solid forms and to use of such solid forms for the therapeutic treatment of warm-blooded animals.
摘要翻译：本发明涉及制备式5化合物或其立体异构体，互变异构体或其盐的方法，其中取代基如说明书中所定义。本发明还涉及用于化合物A及其盐的特定固体形式的这种固体形式的新制备方法，以及这些固体形式用于治疗温血动物的新方法。

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