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1.依法登记的发明7-oxabicycloheptane carboxylic acid prostaglandin analog intermediates useful in the preparation of anti-thrombotic and anti-vasospastic compounds and method for preparing same 失效可用于制备抗血栓形成和抗血管痉挛性化合物的7-氧杂双环庚烷羧酸前列腺素类似物中间体及其制备方法
公开(公告)号：USH1737H
公开(公告)日：1998-06-02
申请号：US828460
申请日：1997-03-28
IPC分类号： C07C237/06 , C07D493/08 , C07D263/52
CPC分类号： C07D493/08 , C07C237/06
摘要： A method is provided for preparing intermediates for 7-oxabicycloheptane carboxylic acid intermediates of the structures ##STR1## wherein R is alkyl, aryl, arylalkyl or cycloalkyl; R.sup.1 is alkyl, arylalkyl or cycloalkyl; R.sup.2 is aryl or arylalkyl; and of the structure ##STR2## where R and R.sup.1 are as defined above, which may be used in making the final anti-thrombotic--anti-vasospastic compounds.
摘要翻译： 提供了制备其中R为烷基，芳基，芳基烷基或环烷基的结构的7-氧杂双环庚烷羧酸中间体的中间体的方法; R1是烷基，芳烷基或环烷基; R2是芳基或芳基烷基; 和结构<IMAGE>，其中R和R 1如上所定义，其可用于制备最终的抗血栓形成 - 抗血管痉挛性化合物。
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公开(公告)号：US06468781B1
公开(公告)日：2002-10-22
申请号：US09510925
申请日：2000-02-22
申请人： Ronald Hanson , Mary Jo Donovan , Steven Goldberg , Paul A. Jass , Wen-Sen Li , Ramesh Patel , Keith Ramig , Laszlo J. Szarka , John J. Venit
发明人： Ronald Hanson , Mary Jo Donovan , Steven Goldberg , Paul A. Jass , Wen-Sen Li , Ramesh Patel , Keith Ramig , Laszlo J. Szarka , John J. Venit
IPC分类号： C12P2106
CPC分类号： C12N9/0018 , C12N9/0008 , C12P7/62 , C12P41/002 , C12P41/006
摘要： Processes for stereoselective enzymatic conversion of certain keto carboxylic acid derivatives to form the corresponding alkylamino acid compounds are described. The invention also concerns an engineered yeast host cell containing recombinant nucleic acid capable of expressing a phenylalanine dehydrogenase, as well as an engineered host cell containing recombinant nucleic acid capable of expressing a phenylalanine dehydrogenase enzyme and nucleic acid capable of expressing a formate dehydrogenase enzyme.
摘要翻译： 描述了某些酮羧酸衍生物立体选择性酶转化以形成相应的烷基氨基酸化合物的方法。 本发明还涉及包含能够表达苯丙氨酸脱氢酶的重组核酸的工程酵母宿主细胞，以及含有能够表达苯丙氨酸脱氢酶的重组核酸和能够表达甲酸脱氢酶的核酸的工程化宿主细胞。
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公开(公告)号：US06486331B2
公开(公告)日：2002-11-26
申请号：US09848464
申请日：2001-05-03
申请人： Ronald L. Hanson , Paul A. Jass , Wen-Sen Li , Ramesh Patel , Keith Ramig , John J. Venit
发明人： Ronald L. Hanson , Paul A. Jass , Wen-Sen Li , Ramesh Patel , Keith Ramig , John J. Venit
IPC分类号： C07D31700
CPC分类号： C12N9/0018 , C12N9/0008 , C12P7/62 , C12P41/002 , C12P41/006
摘要： Substituted alkylketo compounds of the formula can be converted to the corresponding amino acid by a stereoselective enzymatic process. The resulting amino acid compounds can be employed as starting materials for pharmaceutically active compounds. This invention is directed to the substituted alkylketo compounds and their method of preparation.
摘要翻译： 通过立体选择性酶法将公式的取代烷基酮化合物转化成相应的氨基酸。 所得氨基酸化合物可用作药物活性化合物的起始原料。 本发明涉及取代的烷基酮化合物及其制备方法。
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公开(公告)号：US6140088A
公开(公告)日：2000-10-31
申请号：US350428
申请日：1999-07-08
申请人： Ronald Hanson , Mary Jo Donovan , Steven Goldberg , Paul A. Jass , Wen-Sen Li , Ramesh Patel , Keith Ramig , Laszlo J. Szarka , John J. Venit
发明人： Ronald Hanson , Mary Jo Donovan , Steven Goldberg , Paul A. Jass , Wen-Sen Li , Ramesh Patel , Keith Ramig , Laszlo J. Szarka , John J. Venit
IPC分类号： C12N15/09 , C12N1/19 , C12N9/06 , C12P7/62 , C12P13/00 , C12P17/04 , C12P17/06 , C12P41/00 , C12R1/01 , C12R1/84 , C12P9/00
CPC分类号： C12N9/0018 , C12P41/002 , C12P41/006 , C12P7/62
摘要： Processes for stereoselective enzymatic conversion of certain keto carboxylic acid derivatives to form the corresponding alkylamino acid compounds are described. The invention also concerns an engineered yeast host cell containing recombinant nucleic acid capable of expressing a phenylalanine dehydrogenase, as well as an engineered host cell containing recombinant nucleic acid capable of expressing a phenylalanine dehydrogenase enzyme and nucleic acid capable of expressing a formate dehydrogenase enzyme.
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公开(公告)号：US06261810B1
公开(公告)日：2001-07-17
申请号：US09386588
申请日：1999-08-31
申请人： Ramesh N. Patel , Amit Banerjee , Venkata B. Nanduri , Laszlo J. Szarka , Shankar Swaminathan , John J. Venit , Jerome L. Moniot , David A. Lust , Sushil K. Srivastava
发明人： Ramesh N. Patel , Amit Banerjee , Venkata B. Nanduri , Laszlo J. Szarka , Shankar Swaminathan , John J. Venit , Jerome L. Moniot , David A. Lust , Sushil K. Srivastava
IPC分类号： C12P1718
CPC分类号： C07K5/06139 , A61K38/00 , C07K14/8103 , C12N9/1096
摘要： The present invention concerns an enzymatic oxidative deamination process of a dipeptide monomer to prepare an intermediate useful to prepare compounds having endopeptidase and angiotensin converting enzyme inhibition activity.
摘要翻译： 本发明涉及二肽单体的酶氧化脱氨过程，以制备可用于制备具有内肽酶和血管紧张素转化酶抑制活性的化合物的中间体。
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6.发明授权Preparation of [4S-(4.alpha.,7.alpha.,10a.beta.)]-4-amino-octahydro-5-oxo-7H-pyrido[2,1 -b] [1,3]thiazepine-7-carboxylic acid, methyl ester and salts thereof via novel disulfides 有权[4S-（4α，7α，10aβ）] -4-氨基 - 八氢-5-氧代-7H-吡啶并[2,1-b] [1,3]硫氮杂-7-甲酸甲酯 酯及其盐通过新的二硫化物
公开(公告)号：US6162913A
公开(公告)日：2000-12-19
申请号：US349861
申请日：1999-07-08
申请人： Jerome L. Moniot , Sushil K. Srivastava , William J. Winter , John J. Venit , Shankar Swaminathan , Keith Ramig , Paul A. Jass , Mark D. Schwinden , John L. Dillon, Jr. , Saibaba Racha , James Simpson , Chien-Kuang Chen , Shawn K. Pack
发明人： Jerome L. Moniot , Sushil K. Srivastava , William J. Winter , John J. Venit , Shankar Swaminathan , Keith Ramig , Paul A. Jass , Mark D. Schwinden , John L. Dillon, Jr. , Saibaba Racha , James Simpson , Chien-Kuang Chen , Shawn K. Pack
IPC分类号： C07D513/04 , C07B53/00 , C07B61/00 , C07C229/04 , C07C229/22 , C07C261/00 , C07C319/22 , C07C323/59 , C07C323/60 , C07D281/02
CPC分类号： C07D513/04 , C07C323/60 , Y02P20/55
摘要： N-protected-L-homocysteine disulfide of the formula ##STR1## or an activated form thereof is reacted with (S)-2-amino-6,6-dimethoxyhexanoic acid, methyl ester to give the disulfide intermediate of the formula ##STR2## Cleavage of the disulfide bond followed by acid catalyzed cyclization produces the N-protected lactam of formula III which is useful for preparing the pharmaceutically active compound omapatrilat.
摘要翻译： 将下式的N-保护的L-高半胱氨酸二硫化物或其活化形式与（S）-2-氨基-6,6-二甲氧基己酸甲酯反应，得到式的二硫化物中间体 通过酸催化环化产生式III的N-保护的内酰胺，其可用于制备药物活性化合物omapatrilat。
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公开(公告)号：US06515170B1
公开(公告)日：2003-02-04
申请号：US09843226
申请日：2001-04-26
申请人： Ramesh N. Patel , Amit Banerjee , Venkata B. Nanduri , Steven L. Goldberg , Robert M. Johnston , Thomas P. Tully , Laszlo J. Szarka , Shankar Swaminathan , John J. Venit , Jerome L. Moniot , William J. Winter , Neal G. Anderson , David A. Lust , Gerard Crispino , Sushil K. Srivastava
发明人： Ramesh N. Patel , Amit Banerjee , Venkata B. Nanduri , Steven L. Goldberg , Robert M. Johnston , Thomas P. Tully , Laszlo J. Szarka , Shankar Swaminathan , John J. Venit , Jerome L. Moniot , William J. Winter , Neal G. Anderson , David A. Lust , Gerard Crispino , Sushil K. Srivastava
IPC分类号： C07C3200
CPC分类号： C07K5/06139 , A61K38/00 , C07K14/8103 , C12N9/1096
摘要： The present invention concerns an enzymatic oxidative deamination process of a dipeptide monomer to prepare an intermediate useful to prepare compounds having endopeptidase and angiotensin converting enzyme inhibition activity.
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8.发明申请Combretastatin A-4 Phosphate Prodrug Mono- and Di- Organic Amine Salts, Mono- and Di- Amino Acid Salts, and Mono- and Di- Amino Acid Ester Salts 审中-公开Combretastatin A-4磷酸盐前药单 - 和二 - 有机胺盐，单 - 和二 - 氨基酸盐，单 - 和二 - 氨基酸酯盐公开(公告)号：US20090186857A1
公开(公告)日：2009-07-23
申请号：US12265586
申请日：2008-11-05
申请人： John J. Venit , Mandar V. Dali , Manisha M. Dali , Yande Huang , Charles E. Dahlheim , Ravindra W. Tejwani
发明人： John J. Venit , Mandar V. Dali , Manisha M. Dali , Yande Huang , Charles E. Dahlheim , Ravindra W. Tejwani
IPC分类号： A61K31/66
CPC分类号： C07F9/12 , A61K9/0053 , A61K9/28 , A61K31/66
摘要： Provided herein are novel and useful combretastatin A-4 prodrug salts that increase the solubility of combretastatin A-4, readily regenerate combretastatin A-4 in vivo under normal physiological conditions, and which produce physiologically tolerable products as a result of the regeneration of combretastatin A-4.
摘要翻译： 本文提供了新的和有用的考布他汀A-4前药盐，其增加了考布他汀A-4的溶解度，在正常生理条件下容易地在体内再生考布他汀A-4，并且由于考布他汀A的再生而产生生理上可耐受的产物 -4。
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9.发明授权Combretastatin A-4 phosphate prodrug mono- and di-organic amine salts, mono- and di- amino acid salts, and mono- and di-amino acid ester salts 有权Combretastatin A-4磷酸酯前药单 - 和二 - 有机胺盐，单 - 和二 - 氨基酸盐，以及单 - 和二 - 氨基酸酯盐公开(公告)号：US06670344B2
公开(公告)日：2003-12-30
申请号：US09950500
申请日：2001-09-11
申请人： John J. Venit , Mandar V. Dali , Manisha M. Dali , Yande Huang , Charles E. Dahlheim , Ravindra W. Tejwani
发明人： John J. Venit , Mandar V. Dali , Manisha M. Dali , Yande Huang , Charles E. Dahlheim , Ravindra W. Tejwani
IPC分类号： A01N5700
CPC分类号： C07D233/64 , C07C211/14 , C07C215/10 , C07C215/12 , C07C229/08 , C07C229/26 , C07C279/14 , C07F9/12
摘要： Provided herein are novel and useful combretastatin A-4 prodrug salts that increase the solubility of combretastatin A-4, readily regenerate combretastatin A-4 in vivo under normal physiological conditions, and which produce physiologically tolerable products as a result of the regeneration of combretastatin A-4.
摘要翻译： 本文提供了新的和有用的考布他汀A-4前药盐，其增加了考布他汀A-4的溶解度，在正常生理条件下容易地在体内再生考布他汀A-4，并且由于考布他汀A的再生而产生生理上可耐受的产物 -4。
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10.发明授权Combretastatin A-4 phosphate prodrug mono-and di-organic amine salts, mono-and di-amino acid salts, and mono-and di-amino acid ester salts 有权Combretastatin A-4磷酸酯前药单 - 和二 - 有机胺盐，单 - 和二 - 氨基酸盐，以及单 - 和二 - 氨基酸酯盐公开(公告)号：US07659261B2
公开(公告)日：2010-02-09
申请号：US11366105
申请日：2006-03-01
申请人： John J. Venit , Mandar V. Dali , Manisha M. Dali , Yande Huang , Charles E. Dahlheim , Ravindra W. Tejwani
发明人： John J. Venit , Mandar V. Dali , Manisha M. Dali , Yande Huang , Charles E. Dahlheim , Ravindra W. Tejwani
CPC分类号： C07F9/12 , A61K9/0053 , A61K9/28 , A61K31/66
摘要： Provided herein are novel and useful combretastatin A-4 prodrug salts that increase the solubility of combretastatin A-4, readily regenerate combretastatin A-4 in vivo under normal physiological conditions, and which produce physiologically tolerable products as a result of the regeneration of combretastatin A-4.
摘要翻译： 本文提供了新的和有用的考布他汀A-4前药盐，其增加了考布他汀A-4的溶解度，在正常生理条件下容易地在体内再生考布他汀A-4，并且由于考布他汀A的再生而产生生理上可耐受的产物 -4。
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