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1. 再颁专利

USRE40794E1 Crystalline forms of carbapenem antibiotics and methods of preparation 有权
标题翻译：碳青霉烯类抗生素的结晶形式及其制备方法
公开(公告)号：USRE40794E1
公开(公告)日：2009-06-23
申请号：US11999720
申请日：2002-09-20
申请人： Karel M. J. Brands , Raymond Cvetovich , Louis S. Crocker , Michael D. Ward , Amar J. Mahajan , Robert M. Wenslow , John M. Williams , Daniel R. Sidler , Charles Orella , Elizabeth S. Fisher , Ronald Jobson
发明人： Karel M. J. Brands , Raymond Cvetovich , Louis S. Crocker , Michael D. Ward , Amar J. Mahajan , Robert M. Wenslow , John M. Williams , Daniel R. Sidler , Charles Orella , Elizabeth S. Fisher , Ronald Jobson
IPC分类号： C07D477/20
CPC分类号： C07D477/20
摘要： A process for preparing a crystalline, carbapenem monosodium salt of formula IIa: characterized by the steps a) adding about 10 to 30% of an organic solvent to an aqueous solution of the carbapenem, b) cooling the resulting solution to less than −5° C., c) adjusting the pH using a solution containing an acid in an organic solvent to give the appropriate pH for crystallization, and d) crystallizing the compound by adding methanol, and a C2-5 alcohol at between −5 and −25° C.
摘要翻译：制备式IIa的结晶碳青霉烯单钠盐的方法，其特征在于以下步骤：a）向碳青霉烯的水溶液中加入约10至30％的有机溶剂，b）将所得溶液冷却至小于-5℃ c）c）使用在有机溶剂中含有酸的溶液调节pH以得到适当的结晶pH，和d）通过加入甲醇和C2-5醇在-5至-25℃之间使该化合物结晶 C。

2. 发明授权

US07145002B2 Crystalline forms of carbapenem antibiotics and methods of preparation 有权
标题翻译：碳青霉烯类抗生素的结晶形式及其制备方法
公开(公告)号：US07145002B2
公开(公告)日：2006-12-05
申请号：US10485319
申请日：2002-09-20
申请人： Karel M. J. Brands , Raymond Cvetovich , Louis S. Crocker , Michael D. Ward , Amar J. Mahajan , Robert M. Wenslow , John M. Williams , Daniel R. Sidler , Charles Orella , Elizabeth S. Fisher , Ronald Jobson
发明人： Karel M. J. Brands , Raymond Cvetovich , Louis S. Crocker , Michael D. Ward , Amar J. Mahajan , Robert M. Wenslow , John M. Williams , Daniel R. Sidler , Charles Orella , Elizabeth S. Fisher , Ronald Jobson
IPC分类号： C07D477/20
CPC分类号： C07D477/20
摘要： A process for preparing a crystalline, carbapenem monosodium salt of formula IIa: characterized by the steps a) adding about 10 to 30% of an organic solvent to an aqueous solution of the carbapenem, b) cooling the resulting solution to less than −5° C., c) adjusting the pH using a solution containing an acid in an organic solvent to give the appropriate pH for crystallization, and d) crystallizing the compound by adding methanol, and a C2-5 alcohol at between −5 and −25° C.
摘要翻译：制备式IIa的结晶碳青霉烯单钠盐的方法，其特征在于以下步骤：a）向碳青霉烯的水溶液中加入约10至30％的有机溶剂，b）将所得溶液冷却至小于-5℃ c）c）使用在有机溶剂中含有酸的溶液调节pH以得到适当的结晶pH，和d）通过加入甲醇和C 2-5醇来使化合物结晶在-5和-25℃之间

3. 发明授权

US5952323A Carbapenem antibiotic 失效
标题翻译：碳青霉烯类抗生素
公开(公告)号：US5952323A
公开(公告)日：1999-09-14
申请号：US64426
申请日：1998-04-22
申请人： Jeffrey A. Zimmerman , John M. Williams , Paul A. Bergquist , Lisa M. DiMichele , David C. DuBost , Michael J. Kaufman , Daniel R. Sidler , William A. Hunke
发明人： Jeffrey A. Zimmerman , John M. Williams , Paul A. Bergquist , Lisa M. DiMichele , David C. DuBost , Michael J. Kaufman , Daniel R. Sidler , William A. Hunke
IPC分类号： A61K31/40 , C07D20060101 , C07D477/20 , C07D207/16 , C07D403/12
CPC分类号： C07D477/20
摘要： A pharmaceutical composition is disclosed which contains a compound of formula I: ##STR1## or a pharmaceutically acceptable salt, prodrug or hydrate thereof, in the stabilized form and/or in combination with a carbon dioxide source.
摘要翻译：公开了一种药物组合物，其含有稳定形式的和/或与二氧化碳源组合的式I化合物或其药学上可接受的盐，前药或水合物。

4. 发明授权

US06320049B1 Alpha 1a adrenergic receptor antagonists 失效
标题翻译： Alpha 1a肾上腺素能受体拮抗剂
公开(公告)号：US06320049B1
公开(公告)日：2001-11-20
申请号：US09563203
申请日：2000-05-02
申请人： Daniel R. Sidler , Robert D. Larsen , Wenjie Li
发明人： Daniel R. Sidler , Robert D. Larsen , Wenjie Li
IPC分类号： C07D23922
CPC分类号： C07D239/22 , C07D401/04 , C07D401/14
摘要： This invention relates to crystalline pharmaceutically acceptable salts of an alpha 1a adrenergic receptor antagonist, Compound A, which are useful in the treatment of benign prostatic hyperplasia. Pharmaceutical compositions employing the crystalline salts, and processes for making and using the crystalline salts and pharmaceutical compositions of Compound A are also disclosed. This invention further relates to a process for obtaining enantiomerically pure intermediate useful for the synthesis of end product alpha 1a adrenergic receptor antagonists. The end product compounds are useful for the treatment of benign prostatic hyperplasia and for relaxing lower urinary tract tissue. The invention also relates to a process for preparing a class of dihydropyrimidinone compounds of which Compound A is a member, wherein the process involves deprotonating a dihydropyrimidinone compound and then coupling the deprotonated derivative with a primary amine.
摘要翻译：本发明涉及可用于治疗良性前列腺增生的α1α肾上腺素能受体拮抗剂，化合物A的结晶药学上可接受的盐。还公开了使用结晶盐的药物组合物，以及制备和使用化合物A的结晶盐和药物组合物的方法。本发明还涉及用于获得可用于合成终产物α1α肾上腺素能受体拮抗剂的对映体纯中间体的方法。最终产品化合物可用于治疗良性前列腺增生和放松下尿路组织。本发明还涉及一种制备其中化合物A为成员的一类二氢嘧啶酮化合物的方法，其中该方法包括使二氢嘧啶酮化合物去质子化，然后将去质子化衍生物与伯胺偶联。

5. 发明授权

US06372911B1 Process for preparing &bgr;-hydroxycarbamates and their conversion to oxazolidinones 失效
标题翻译：制备β-羟基氨基甲酸酯及其转化为恶唑烷酮的方法
公开(公告)号：US06372911B1
公开(公告)日：2002-04-16
申请号：US09482799
申请日：2000-01-13
申请人： Nancy Barta , Robert D. Larsen , Daniel R. Sidler , Steven A. Weissman
发明人： Nancy Barta , Robert D. Larsen , Daniel R. Sidler , Steven A. Weissman
IPC分类号： C07D41312
CPC分类号： C07D413/12 , C07C271/16 , C07D211/18 , C07D263/38
摘要： A process for preparing a &bgr;-hydroxy carbamate product is disclosed. The process comprises reacting an olefin compound containing at least one carbon-carbon double bond with a carbamate in an aqueous solvent and in the presence of a base, an osmium catalyst, a co-oxidant selected from a halohydantoin, a haloisocyanuric acid, and an alkali metal salt of a haloisocyanuric acid, and optionally an asymmetric ligand, to form a reaction mixture containing the &bgr;-hydroxy carbamate product. The process optionally further comprises treating the &bgr;-hydroxy carbamate product with additional base to form an oxazolidinone. The oxazolidinones are useful as chiral auxiliary agents and as intermediates for the formation of pharmaceutically active substances such as alpha 1 a adrenergic receptor antagonists. A process for preparing nitrogen-functionalized derivatives of the oxazolidinones is also disclosed.
摘要翻译：公开了一种制备β-羟基氨基甲酸酯产物的方法。该方法包括使含有至少一个碳 - 碳双键的烯烃化合物与氨基甲酸酯在水溶剂中反应，并在碱，锇催化剂，选自卤代乙内酰脲，卤代异氰脲酸和卤代异氰尿酸的碱金属盐和任选的不对称配体，以形成含有β-羟基氨基甲酸酯产物的反应混合物。该方法任选地还包括用另外的碱处理β-羟基氨基甲酸酯产物以形成恶唑烷酮。恶唑烷酮可用作手性助剂，也可用作形成药物活性物质如α1肾上腺素能受体拮抗剂的中间体。还公开了制备恶唑烷酮的氮官能化衍生物的方法。

6. 发明授权

US06207444B1 Enzymatic process of making alpha 1a adrenergic receptor antagonists using protease 失效
标题翻译：使用蛋白酶制备α1a肾上腺素能受体拮抗剂的酶学方法
公开(公告)号：US06207444B1
公开(公告)日：2001-03-27
申请号：US09122301
申请日：1998-07-24
申请人： Daniel R. Sidler , Michel Chartrain , Norihiro Ikemoto , Gerald F. Bills , Christopher Roberge , Colleen S. Taylor
发明人： Daniel R. Sidler , Michel Chartrain , Norihiro Ikemoto , Gerald F. Bills , Christopher Roberge , Colleen S. Taylor
IPC分类号： C12P1712
CPC分类号： C07D239/22 , C07D401/04 , C07D401/14
摘要： This invention relates to crystalline pharmaceutically acceptable salts of an alpha 1a adrenergic receptor antagonist, Compound A, which are useful in the treatment of benign prostatic hyperplasia. Pharmaceutical compositions employing the crystalline salts, and processes for making and using the crystalline salts and pharmaceutical compositions of Compound A are also disclosed. This invention further relates to a process for obtaining enantiomerically pure intermediate useful for the synthesis of end product alpha 1a adrenergic receptor antagonists. The end product compounds are useful for the treatment of benign prostatic hyperplasia and for relaxing lower urinary tract tissue. The invention also relates to a process for preparing a class of dihydropyrimidinone compounds of which Compound A is a member, wherein the process involves deprotonating a dihydropyrimidinone compound and then coupling the deprotonated derivative with a primary amine.
摘要翻译：本发明涉及可用于治疗良性前列腺增生的α1α肾上腺素能受体拮抗剂，化合物A的结晶药学上可接受的盐。还公开了使用结晶盐的药物组合物，以及制备和使用化合物A的结晶盐和药物组合物的方法。本发明还涉及用于获得可用于合成终产物α1α肾上腺素能受体拮抗剂的对映体纯中间体的方法。最终产品化合物可用于治疗良性前列腺增生和放松下尿路组织。本发明还涉及一种制备其中化合物A为成员的一类二氢嘧啶酮化合物的方法，其中该方法包括使二氢嘧啶酮化合物去质子化，然后将去质子化衍生物与伯胺偶联。

7. 发明授权

US5786472A Process for making dihydropyrimidinones 失效
标题翻译：制备二氢嘧啶酮的方法
公开(公告)号：US5786472A
公开(公告)日：1998-07-28
申请号：US766400
申请日：1996-12-12
申请人： Essa Hsinyi Hu , Daniel R. Sidler , Ulf H. Dolling , Michael A. Patane
发明人： Essa Hsinyi Hu , Daniel R. Sidler , Ulf H. Dolling , Michael A. Patane
IPC分类号： C07D239/22 , C07D239/36
CPC分类号： C07D239/22
摘要： The present invention provides a process for forming 5-(alkyl or alkoxy)carbonyl-6-alkyl-4-(aryl or alkyl)-3,4-2(1H)-dihydropyrimidinones by combining a .beta.-keto ester or diketone, an aldehyde and urea in the presence of a boron reagent, a metal salt (e.g., Cu.sub.2 O) and a catalyst (e.g., acid). The reaction is typically run in one pot in a solvent to afford dihydropyrimidinones in higher yields and with easier work up than previously known methods.
摘要翻译：本发明提供了通过将β-酮酯或二酮组合形成5-（烷基或烷氧基）羰基-6-烷基-4-（芳基或烷基）-3,4-2（1H） - 二氢嘧啶酮的方法，醛和尿素在硼试剂，金属盐（例如Cu 2 O）和催化剂（例如酸）的存在下进行。反应通常在溶剂中在一锅中进行，以更高的产率提供二氢嘧啶酮，并且比以前已知的方法更容易处理。

8. 发明授权

US06320052B1 Process for the preparation of leukotriene antagonists 有权
标题翻译：白三烯拮抗剂的制备方法
公开(公告)号：US06320052B1
公开(公告)日：2001-11-20
申请号：US09274062
申请日：1999-03-22
申请人： Mahadevan Bhupathy , Daniel R. Sidler , James M. McNamara , Ralph P. Volante , James Bergan
发明人： Mahadevan Bhupathy , Daniel R. Sidler , James M. McNamara , Ralph P. Volante , James Bergan
IPC分类号： A61K3147
CPC分类号： C07D215/14 , C07C323/53 , C07C2601/02
摘要： The present invention relates to a process for the preparation of a compound of formula (I) or a sodium salt thereof wherein HET is 7-chloroquinolin-2-yl or 6,7-difluoroquinolin-2-yl, which comprises: reacting the dilithium dianion of 1-(mercapto-methyl)cyclopropaneacetic acid with a compound of formula (II) wherein HET is as defined above and L is arylsulfonyl or alkylsulfonyl. The invention further provides the dicyclohexylamine salt of a compound of formula (I).
摘要翻译：本发明涉及制备式（I）化合物或其钠盐的方法，其中HET是7-氯喹啉-2-基或6,7-二氟喹啉-2-基，其包括：使二锂二阴离子的1-（巯基 - 甲基）环丙烷乙酸与式（II）化合物反应，其中HET如上定义，L是芳基磺酰基或烷基磺酰基。本发明还提供式（I）化合物的二环己基胺盐。

9. 发明授权

US5614632A Process for the preparation of leukotriene anatgonists 失效
标题翻译：白三烯阴离子药物的制备方法
公开(公告)号：US5614632A
公开(公告)日：1997-03-25
申请号：US439733
申请日：1995-05-12
申请人： Mahadevan Bhupathy , James M. McNamara , Daniel R. Sidler , Ralph P. Volante , James Bergan
发明人： Mahadevan Bhupathy , James M. McNamara , Daniel R. Sidler , Ralph P. Volante , James Bergan
IPC分类号： C07D215/18 , A61K31/47 , A61P11/06 , C07C215/14 , C07C313/02 , C07C323/53 , C07D215/12 , C07D215/14
CPC分类号： C07D215/14 , C07C323/53 , C07C2101/02
摘要： The present invention relates to a process for the preparation of a compound of formula (I) or a sodium salt thereof ##STR1## wherein HET is 7-chloroquinolin-2-yl or 6,7-difluoroquinolin-2-yl, which comprises: reacting the dilithium dianion of 1-(mercaptomethyl)cyclopropaneacetic acid with a compound of formula (II) ##STR2## wherein HET is as defined above and L is arylsulfonyl or alkylsulfonyl. The invention further provides the dicyclohexylamine salt of a compound of formula (I).
摘要翻译：本发明涉及制备式（I）化合物或其钠盐的方法，其中HET是7-氯喹啉-2-基或6,7-二氟喹啉-2-基，其包括：使1-（巯基甲基）环丙烷乙酸的二锂二阴离子与式（II）化合物（II）反应，其中HET如上所定义，L是芳基磺酰基或烷基磺酰基。本发明还提供式（I）化合物的二环己基胺盐。

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