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![Process for the preparation of [(1R), 2S]-2-aminopropionic acid 2-[4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[2, 1-F][1,2,4]triazin-6-yloxy]-1-methylethyl ester](/abs-image/US/2010/03/02/US07671199B2/abs.jpg.150x150.jpg)
1.发明授权Process for the preparation of [(1R), 2S]-2-aminopropionic acid 2-[4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[2, 1-F][1,2,4]triazin-6-yloxy]-1-methylethyl ester 有权制备[（1R），2S] -2-氨基丙酸2- [4-（4-氟-2-甲基-1H-吲哚-5-基氧基）-5-甲基吡咯并[2,1-F] [1,2,4]三嗪-6-基氧基] -1-甲基乙基酯公开(公告)号：US07671199B2
公开(公告)日：2010-03-02
申请号：US11737787
申请日：2007-04-20
申请人： Gerard A. Crispino , Mourad Hamedi , Thomas L. LaPorte , John E. Thornton , Jaan A. Pesti , Zhongmin Xu , Paul C. Lobben , David K. Leahy , Jale Muslehiddinoglu , Chiajen Lai , Lori Ann Spangler , Robert P. Discordia , Francis S. Gibson
发明人： Gerard A. Crispino , Mourad Hamedi , Thomas L. LaPorte , John E. Thornton , Jaan A. Pesti , Zhongmin Xu , Paul C. Lobben , David K. Leahy , Jale Muslehiddinoglu , Chiajen Lai , Lori Ann Spangler , Robert P. Discordia , Francis S. Gibson
IPC分类号： C07D487/04 , A61K31/53 , A61P3/10
CPC分类号： C07D487/04
摘要： The invention relates to an improved process for preparing [(1R), 2S]-2-aminopropionic acid 2-[4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy]-1-methylethyl ester of the formula: Compound I has been shown to be useful for the treatment of certain types of cancer.
摘要翻译： 本发明涉及制备[（1R），2S] -2-氨基丙酸2- [4-（4-氟-2-甲基-1H-吲哚-5-基氧基）-5-甲基吡咯并[2， 1-f] [1,2,4]三嗪-6-基氧基] -1-甲基乙基酯：化合物I已经显示可用于治疗某些类型的癌症。
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2.发明授权
公开(公告)号：US6022977A
公开(公告)日：2000-02-08
申请号：US47555
申请日：1998-03-25
申请人： Lin-Hua Zhang , Luigi Anzalone , Jaan A. Pesti , Jianguo Yin
发明人： Lin-Hua Zhang , Luigi Anzalone , Jaan A. Pesti , Jianguo Yin
IPC分类号： A61P7/02 , A61P43/00 , C07D261/04 , C12P17/14 , C12P41/00
CPC分类号： C12P17/14 , C07D261/04 , C12P41/005
摘要： The present invention relates generally to a novel method for preparation of substituted isoxazolin-5-yl acetic acid in high optical purity from a stereoisomeric mixture of an esterified substituted isoxazolin-5-yl acetate. The products are useful in the synthesis of compounds for pharmaceuticals, especially the treatment of thrombolytic disorders, and agricultural products.
摘要翻译： 本发明一般涉及由酯化的取代的异恶唑啉-5-基乙酸酯的立体异构体混合物制备高光学纯度的取代的异恶唑啉-5-基乙酸的新方法。 该产品可用于药物化合物的合成，特别是治疗血栓溶解症和农产品。
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公开(公告)号：US06306886B1
公开(公告)日：2001-10-23
申请号：US09094944
申请日：1998-06-15
申请人： Michael Blaise Maurin , Philip Ma , David John Meloni , Jaan A. Pesti , Lucius Thomas Rossano , Randall K. Ward , Jianguo Yin , Lin Hua Zhang , Goss S. Kauffman
发明人： Michael Blaise Maurin , Philip Ma , David John Meloni , Jaan A. Pesti , Lucius Thomas Rossano , Randall K. Ward , Jianguo Yin , Lin Hua Zhang , Goss S. Kauffman
IPC分类号： A61K3112
CPC分类号： C07D261/04
摘要： The potent platelet glycoprotein IIb/IIIa antagonist, roxifiban, is produced in crystalline form. Crystalline roxifiban exists in two polymorphic forms, designated Form 1 and Form 2. These polymorphic forms are characterized by x-ray powder diffraction and solid-state carbon NMR. Pharmaceutical compositions and methods for the treatment or prevention of diseases mediated by platelet aggregation are described.
摘要翻译： 有效的血小板糖蛋白IIb / IIIa拮抗剂罗昔西芬以结晶形式生产。 结晶罗西非酮以两种多晶型形式存在，称为形式1和形式2.这些多晶型以X-射线粉末衍射和固态碳核磁共振为特征。 描述了用于治疗或预防血小板聚集介导的疾病的药物组合物和方法。
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![Process for the preparation of pyrazolo[1,5-a]-1,3,5-triazines and intermediates thereof](/abs-image/US/2008/10/28/US07442792B2/abs.jpg.150x150.jpg)
4.发明授权Process for the preparation of pyrazolo[1,5-a]-1,3,5-triazines and intermediates thereof 有权制备吡唑并[1,5-a] -1,3,5-三嗪的方法及其中间体公开(公告)号：US07442792B2
公开(公告)日：2008-10-28
申请号：US11717440
申请日：2007-03-13
IPC分类号： C07D487/04 , A61K31/53 , A61P3/04 , A61P9/12 , A61P25/22
CPC分类号： C07D231/38 , C07D487/04
摘要： The present invention provides novel processes and intermediates for preparing corticotropin releasing factor (CRF) receptor antagonists having the structure below which are useful in treating CRF-related disorders such as anxiety and depression.
摘要翻译： 本发明提供了用于制备具有以下结构的促肾上腺皮质激素释放因子（CRF）受体拮抗剂的新方法和中间体，其可用于治疗CRF相关疾病如焦虑和抑郁。
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![Processes for the preparation of pyrazolo[1,5-a]-1,3,5-triazines and intermediates thereof](/abs-image/US/2007/04/24/US07208596B2/abs.jpg.150x150.jpg)
5.发明授权Processes for the preparation of pyrazolo[1,5-a]-1,3,5-triazines and intermediates thereof 有权制备吡唑并[1,5-a] -1,3,5-三嗪的方法及其中间体公开(公告)号：US07208596B2
公开(公告)日：2007-04-24
申请号：US10985236
申请日：2004-11-10
CPC分类号： C07D231/38 , C07D487/04
摘要： The present invention provides novel processes and intermediates for preparing corticotropin releasing factor (CRF) receptor antagonists having the structure below which are useful in treating CRF-related disorders such as anxiety and depression
摘要翻译： 本发明提供了用于制备具有以下结构的促肾上腺皮质激素释放因子（CRF）受体拮抗剂的新方法和中间体，其可用于治疗CRF相关病症如焦虑和抑郁
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6.发明授权Enantioselective enzymatic aminolysis of a racemic 2-isoxazolylacetate alkyl ester 失效外消旋2-异恶唑乙酸烷基酯的对映选择性酶解公开(公告)号：US06624311B2
公开(公告)日：2003-09-23
申请号：US10039972
申请日：2001-10-25
申请人： Robert DiCosimo , Philip Ma , Jaan A. Pesti
发明人： Robert DiCosimo , Philip Ma , Jaan A. Pesti
IPC分类号： C07D26104
CPC分类号： C12P41/001 , C07D261/04 , C12P17/14
摘要： The present invention relates to a process for the enantioselective enzymatic aminolysis of racemic 2-[3-(4-cyanophenyl)-4,5-dihydro-5-isoxazolyl]acetate ((R/S)-I) by methyl N&agr;-Boc-L-&agr;,&bgr;-diaminoproprionate.p-toluenesulfonic acid. More specifically, this invention pertains to a process for the enantioselective enzymatic aminolysis of racemic isobutyl 2-[3-(4-cyanophenyl)-4,5-dihydro-5-isoxazolyl]-acetate by methyl N&agr;-Boc-L-&agr;,&bgr;-diaminoproprionate.p-toluene sulfonic acid to produce (R)-methyl-3-[[[3-(4-cyanophenyl)-4,5-dihydro-5-isoxazolyl]acetyl]amino]-N-(butoxycarbonyl)-L-alanine, an intermediate in the preparation of roxifiban, an isoxazoline-based platelet glycoprotein IIb/IIIa antagonist which has activity as an antithrombotic agent.
摘要翻译： 本发明涉及外消旋的2- [3-（4-氰基苯基）-4,5-二氢-5-异恶唑基]乙酸酯（（R / S）-I）的对映选择性酶促氨基化方法由Nalpha-Boc -L-α，β-二氨基丙酸酯对甲苯磺酸。 更具体地，本发明涉及通过Nalpha-Boc-L-α甲基对外消旋异丁基2- [3-（4-氰基苯基）-4,5-二氢-5-异恶唑基] - 乙酸酯的对映选择性酶解的方法， （R） - 甲基-3 - [[[3-（4-氰基苯基）-4,5-二氢-5-异恶唑基]乙酰基]氨基] -N-（丁氧基羰基） L-丙氨酸，罗非昔布的制备中间体，一种具有作为抗血栓形成剂活性的异恶唑啉类血小板糖蛋白IIb / IIIa拮抗剂。
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7.发明授权Crystalline 10,10-Bis((2-fluoro-4-pyridinyl)methyl)-9(10H)-Anthracenone and an improved process for preparing the same 有权结晶10,10-双（（2-氟-4-吡啶基）甲基）-9（10H） - 蒽并酮及其制备方法公开(公告)号：US06214847B1
公开(公告)日：2001-04-10
申请号：US09131953
申请日：1998-08-11
IPC分类号： A61K3144
CPC分类号： C07D213/61
摘要： The present invention relates to processes for the synthesis of a crystalline polymorph of 10,10-Bis((2-fluoro-4-pyridinyl)methyl)-9(10H)-Anthracenone in high purity. The product is useful in the synthesis of pharmaceutical compounds for the reduction of cholinergic system dysfunction.
摘要翻译： 本发明涉及高纯度合成10,10-双（（2-氟-4-吡啶基）甲基）-9（10H） - 蒽酮的结晶多晶型物的方法。 该产品可用于合成用于降低胆碱能系统功能障碍的药物化合物。
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