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公开(公告)号：US08329696B2
公开(公告)日：2012-12-11
申请号：US12749486
申请日：2010-03-29
Applicant: Gideon Pilarski , Nurit Perlman , Ariel Mittelman , Nada Kosutic Hulita , Marina Kalujny , Revital Ramaty
Inventor： Gideon Pilarski , Nurit Perlman , Ariel Mittelman , Nada Kosutic Hulita , Marina Kalujny , Revital Ramaty
IPC: A61K31/495
CPC classification number: C07D487/04
Abstract: Solid state forms of Sitagliptin salts (e.g. Sitagliptin sulfate, Formula I), processes for preparing the solid state forms, and pharmaceutical compositions thereof, are provided. These compounds are of a class of dipeptidyl peptidase IV enzyme inhibitors which are useful, for example, for the manufacture of a medicament for the treatment of type 2 diabetes mellitus.
Abstract translation: 提供西他列汀盐（例如硫酸西替他嗪，式I）的固体形式，制备固体形式的方法及其药物组合物。 这些化合物是一类二肽基肽酶IV酶抑制剂，其可用于例如制备用于治疗2型糖尿病的药物。
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公开(公告)号：US20090099365A1
公开(公告)日：2009-04-16
申请号：US12218401
申请日：2008-07-14
Applicant: Nurit Perlman , Gideon Pilarski
Inventor： Nurit Perlman , Gideon Pilarski
IPC: C07D453/04
CPC classification number: C07D453/02
Abstract: Processes for preparing solifenacin comprising distilling ethanol and organic solvent from a reaction mixture and recycling the organic solvent are described. Also described are processes for reducing solifenacin diastereomeric and enantiomeric impurities.
Abstract translation: 描述了制备索非那新的方法，其包括从反应混合物中蒸馏出乙醇和有机溶剂并回收有机溶剂。 还描述了降低索非那新非对映体和对映异构体杂质的方法。
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公开(公告)号：US20090192326A1
公开(公告)日：2009-07-30
申请号：US12291925
申请日：2008-11-13
Applicant: Nurit Perlman , Marina Etinger , Valerie Niddam-Hildesheim , Mili Abramov
Inventor： Nurit Perlman , Marina Etinger , Valerie Niddam-Hildesheim , Mili Abramov
IPC: C07C229/34
CPC classification number: C07C227/32 , C07C229/34
Abstract: Intermediate compounds in the synthesis of Sitagliptin, 3-amino-4-(2,4,5-trifluorophenyl)but-2-enoic acid alkyl ester, and amino protected-3-amino-4-(2,4,5-trifluorophenyl)but-2-enoic acid alkyl ester, and the stereoselective reduction of these compound to give Synthon I, or the amino-protected Synthon I, are provided.
Abstract translation: 西他列汀，3-氨基-4-（2,4,5-三氟苯基）丁-2-烯酸烷基酯和氨基被保护的3-氨基-4-（2,4,5-三氟苯基） ）丁-2-烯酸烷基酯，并且提供这些化合物的立体选择性还原以产生Synthon I或氨基保护的Synthon I。
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4.发明申请Fluvastatin sodium crystal forms, processes for preparing them, compositions containing them and methods of using them 失效氟伐他汀钠晶体形式，其制备方法，含有它们的组合物和使用它们的方法公开(公告)号：US20080146817A1
公开(公告)日：2008-06-19
申请号：US11699659
申请日：2007-01-29
Applicant: Revital Lifshitz-Liron , Tamas Koltai , Judith Aronhime , Nurit Perlman , Sharon Avhar-Maydan
Inventor： Revital Lifshitz-Liron , Tamas Koltai , Judith Aronhime , Nurit Perlman , Sharon Avhar-Maydan
IPC: C07D209/04
CPC classification number: C07D209/12 , C07D209/24
Abstract: Provided are crystalline forms of fluvastatin sodium and processes for their preparation.
Abstract translation: 提供氟伐他汀钠的结晶形式及其制备方法。
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5.发明授权Fluvastatin sodium crystal forms XIV, LXXIII, LXXIX, LXXX and LXXXVII, processes for preparing them, compositions containing them and methods of using them 失效氟伐他汀钠晶体形成XIV，LXXIII，LXXIX，LXXX和LXXXVII，制备它们的方法，含有它们的组合物和使用它们的方法公开(公告)号：US07368468B2
公开(公告)日：2008-05-06
申请号：US10871916
申请日：2004-06-18
Applicant: Revital Lifshitz-Liron , Tamas Koltai , Judith Aronhime , Nurit Perlman
Inventor： Revital Lifshitz-Liron , Tamas Koltai , Judith Aronhime , Nurit Perlman
IPC: A61K31/40 , C07D209/12
CPC classification number: C07D209/24
Abstract: Provided are polymorphic forms of fluvastatin sodium and processes for their preparation.
Abstract translation: 提供氟伐他汀钠的多晶型物质及其制备方法。
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Patent Agency Ranking
6.发明申请Fluvastatin sodium crystal forms XIV, LXXIII, LXXIX, LXXX and LXXXVII, processes for preparing them, compositions containing them and methods of using them 失效氟伐他汀钠晶体形成XIV，LXXIII，LXXIX，LXXX和LXXXVII，制备它们的方法，含有它们的组合物和使用它们的方法公开(公告)号：US20050038114A1
公开(公告)日：2005-02-17
申请号：US10871916
申请日：2004-06-18
Applicant: Revital Lifshitz-Liron , Tamas Koltai , Judith Aronhime , Nurit Perlman
Inventor： Revital Lifshitz-Liron , Tamas Koltai , Judith Aronhime , Nurit Perlman
IPC: C07D209/24 , C07C69/66 , A61K31/225
CPC classification number: C07D209/24
Abstract: Provided are polymorphic forms of fluvastatin sodium and processes for their preparation.
Abstract translation: 提供氟伐他汀钠的多晶型物质及其制备方法。
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公开(公告)号：US20100041885A1
公开(公告)日：2010-02-18
申请号：US12410738
申请日：2009-03-25
Applicant: Nurit Perlman , Revital Ramaty , Mili Abramov , Nina Finkelstein , Eli Lancry , Shay Asis , Ariel Mittelman
Inventor： Nurit Perlman , Revital Ramaty , Mili Abramov , Nina Finkelstein , Eli Lancry , Shay Asis , Ariel Mittelman
IPC: C07D471/08
CPC classification number: C07D487/04
Abstract: A Sitagliptin phosphate characterized by data selected from the group consisting of: a powder XRD pattern with peaks at 4.7, 13.5, 17.7, 18.3, and 23.7±0.2 degrees two theta; a powder XRD pattern with peaks at about 4.7, 13.5, and 15.5±0.2 degrees two theta and at least another two peaks selected from the following list: 14.0, 14.4, 18.3, 19.2, 19.5 and 23.7±0.2 degrees two theta; and a powder XRD pattern with peaks at about 13.5, 19.2, and 19.5±0.2 degrees two theta and at least another two peaks selected from the following list: 4.7, 14.0, 15.1, 15.5, 18.3, and 18.7±0.2 degrees two theta; a powder XRD pattern with peaks at about 13.5, 15.5, 19.2, 23.7, and 24.4±0.2 degrees two theta; and a powder XRD pattern with peaks at about 4.65, 13.46, 17.63, 18.30, and 23.66±0.10 degrees two theta, processes for preparing said Sitagliptin crystalline form, and pharmaceutical compositions thereof, are provided.
Abstract translation: 磷酸西他列汀，其特征在于选自以下的数据：粉末XRD图谱，其峰为4.7,13.5,17.7,18.3和23.7±0.2度2θ; 在约4.7,13.5和15.5±0.2度2θ处具有峰的粉末XRD图案和至少另外两个选自以下列表的峰：14.0,14.4,18.3,19.2,19.5和23.7±0.2度2θ; 和具有在约13.5,19.2和19.5±0.2度2θ处以及从下列列表中选择的至少另外两个峰的峰的粉末XRD图：4.7,14.0,15.1,15.5,18.3和18.7±0.2度2θ; 在约13.5,15.5,19.2,23.7和24.4±0.2度2θ处具有峰的粉末XRD图案; 并且提供了在约4.65,13.46,17.63,18.30和23.66±0.10度2θ处具有峰的粉末XRD图案，制备所述西格列汀结晶形式的方法及其药物组合物。
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公开(公告)号：US07501448B2
公开(公告)日：2009-03-10
申请号：US11250267
申请日：2005-10-13
Applicant: Nurit Perlman , Eyal Gilboa
Inventor： Nurit Perlman , Eyal Gilboa
IPC: A61K31/4184 , C07D235/04
CPC classification number: C07D235/14 , C07D235/18
Abstract: Provided are processes for preparing telmisartan alkyl ester and telmisartan using environmentally friendly organic solvents that are easily removed from the reaction mixture, wherein a telmisartan alkyl ester is isolated and hydrolyzed to form telmisartan or the telmisartan is prepared using a synthesis in a single reaction vessel.
Abstract translation: 提供了使用易于从反应混合物中除去的环境友好的有机溶剂来制备替米沙坦烷基酯和替米沙坦的方法，其中分离并水解替米沙坦烷基酯以形成替米沙坦，或者在单个反应容器中使用合成制备替米沙坦。
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公开(公告)号：US20080200532A1
公开(公告)日：2008-08-21
申请号：US12150061
申请日：2008-04-23
Applicant: Revital Lifshitz-Liron , Tamas Koltai , Judith Aronhime , Nurit Perlman
Inventor： Revital Lifshitz-Liron , Tamas Koltai , Judith Aronhime , Nurit Perlman
IPC: A61K31/403 , C07D209/02 , A61P7/00
CPC classification number: C07D209/24
Abstract: Provided are polymorphic forms of fluvastatin sodium and processes for their preparation.
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10.发明申请Processes for optical resolution of 1-phenyl-1,2,3,4-tetrahydroisoquinoline 审中-公开1-苯基-1,2,3,4-四氢异喹啉的光学拆分方法公开(公告)号：US20080091023A1
公开(公告)日：2008-04-17
申请号：US11890289
申请日：2007-08-03
Applicant: Nurit Perlman , Tamar Nidam
Inventor： Nurit Perlman , Tamar Nidam
IPC: C07D217/02 , C07D401/14
CPC classification number: C07D453/02 , C07D217/02
Abstract: Optically pure 1(S)-phenyl-1,2,3,4-tetrahydroisoquinoline tartrate is prepared. The 1(S)-phenyl-1,2,3,4-tetrahydroisoquinoline tartrate is particularly useful for preparing solifenacin succinate.
Abstract translation: 制备光学纯的1（S） - 苯基-1,2,3,4-四氢异喹啉酒石酸盐。 1（S） - 苯基-1,2,3,4-四氢异喹啉酒石酸盐特别适用于制备琥珀酸索非那新。
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