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1. 发明申请

US20060160785A1 Ezetimibe polymorphs 审中-公开
标题翻译：依泽替米贝多晶型物
公开(公告)号：US20060160785A1
公开(公告)日：2006-07-20
申请号：US11295141
申请日：2005-12-05
申请人： Judith Aronhime , Tamas Koltai , Guy Samburski , Ori Lerman , Reuven Izsak
发明人： Judith Aronhime , Tamas Koltai , Guy Samburski , Ori Lerman , Reuven Izsak
IPC分类号： A61K31/397 , C07D205/02
CPC分类号： C07D205/08
摘要： Provided are processes for preparing crystalline forms of ezetimibe, such as ezetimibe Form A or Form B, for example, by precipitating ezetimibe from selected solvents. Alternatively, some forms may be transformed into different forms at elevated temperatures or under various humidity conditions, or by micronization. Also provided are micronized ezetimibe Form A, micronized ezetimibe Form B, and ezetimibe having a plate morphology. Pharmaceutical compositions containing these forms are particularly useful in reducing cholesterol in patients in need thereof.
摘要翻译：提供了制备依泽替米贝的结晶形式的方法，例如依泽替米贝形式A或B型，例如通过从选择的溶剂中沉淀依泽替米贝。或者，一些形式可以在升高的温度或在各种湿度条件下或通过微粉化转化成不同的形式。还提供了微粒化的依泽替米贝形式A，微粉化的依泽替米贝形式B和具有平板形态的依泽替米贝。含有这些形式的药物组合物特别可用于降低有需要的患者的胆固醇。

2. 发明申请

US20050215791A1 Process for preparing aripiprazole 审中-公开
标题翻译：阿立哌唑的制备方法
公开(公告)号：US20050215791A1
公开(公告)日：2005-09-29
申请号：US11053645
申请日：2005-02-07
申请人： Ben-Zion Dolitzky , Ori Lerman
发明人： Ben-Zion Dolitzky , Ori Lerman
IPC分类号： C07D215/22 , C07D215/227 , C07D43/02
CPC分类号： C07D215/227
摘要： The invention encompasses the synthesis of aripiprazole from BBQ and DCP, and comprises mixing 7-(4-bromobutoxy)-3,4-dihydrocarbostyril (BBQ) and 1-(2,3-dichlorophenyl)piperazine hydrochloride (DCP) in the presence of at least one base and at least one organic solvent to form a reaction mixture; heating the reaction mixture for a sufficient amount of time to effect the reaction; and isolating aripiprazole. The invention also encompasses the use of phase transfer catalysts in synthesizing aripiprazole from BBQ and DCP.
摘要翻译：本发明包括从BBQ和DCP合成阿立哌唑，并包括在存在下混合7-（4-溴丁氧基）-3,4-二氢喹诺酮（BBQ）和1-（2,3-二氯苯基）哌嗪盐酸盐（DCP）至少一种碱和至少一种有机溶剂以形成反应混合物; 加热反应混合物足够的时间以进行反应; 并分离阿立哌唑。本发明还包括使用相转移催化剂从BBQ和DCP合成阿立哌唑。

3. 发明授权

US4954648A Method for the bromination of aromatic compound 失效
标题翻译：芳香族化合物溴化方法
公开(公告)号：US4954648A
公开(公告)日：1990-09-04
申请号：US350394
申请日：1989-05-11
申请人： Ori Lerman , Shlomo Rozen
发明人： Ori Lerman , Shlomo Rozen
IPC分类号： C07B39/00 , C07C17/12 , C07C201/12 , C07C205/12 , C07C205/45 , C07C255/50
CPC分类号： C07C255/50 , C07B39/00 , C07C17/12 , C07C201/12
摘要： A method for the bromination of aromatic compounds, including substituted deactivated aromatic compounds, at mild temperature conditions is disclosed. The method comprises reacting an aromatic compound with a bromination agent consisting of bromine-trifluoride and bromine at a temperature ranging between -10.degree. C. and 30.degree. C. The bromination reaction takes place instantaneously and the brominated aromatic compound is separated from the original reactant by known organic chemistry techniques.

4. 发明授权

US06747163B2 Method for the isolation of 6&agr;, 9&agr;-difluoro-11&bgr;, 17&agr;-dihydroxy-16&agr;-methylpregna-3-oxo-1,4-diene-17&bgr;-carboxylic acid 失效
标题翻译：分离6α，9α-二氟-11βa，17α-二羟基-16α-甲基孕酮-3-氧代-1,4-二烯-17β-羧酸的方法
公开(公告)号：US06747163B2
公开(公告)日：2004-06-08
申请号：US10406445
申请日：2003-04-04
申请人： Yaacov Rubinsztain , Ariana Segal , Joseph Kaspi , Ori Lerman
发明人： Yaacov Rubinsztain , Ariana Segal , Joseph Kaspi , Ori Lerman
IPC分类号： C07C5022
CPC分类号： C07J3/00
摘要： The invention provides a process for the preparation and isolation of compound of formula 2, comprising the following steps: oxidizing Flumethasone dissolved in a tetrahydrofuran-water mixture with periodic acid at a temperature lower than 30° C.; cooling the reaction mixture to a temperature lower than 10° C.; adding an antisolvent precooled to a temperature lower than 10° C.; and separating the precipitated crystal by filtration, whereby there is obtained a compound of formula 2 in a yield of at least 98% and of a chromatographic purity of at least 99%.
摘要翻译：本发明提供了制备和分离式2化合物的方法，包括以下步骤：在低于30℃的温度下，用溶解于四氢呋喃 - 水混合物中的氟康萨坦用高碘酸氧化。将反应混合物冷却至低于10℃的温度; 加入预冷至低于10℃的抗溶剂; 并通过过滤分离沉淀的晶体，由此获得式2的化合物，产率至少为98％，色谱纯度为至少99％。

5. 发明授权

US5672755A Process for the purification of (RR-SS)-2-dimethyl-aminomethyl-1-(3-methoxyphenyl)cyclohexanol and its salts 失效
标题翻译：纯化（RR-SS）-2-二甲基 - 氨基甲基-1-（3-甲氧基苯基）环己醇及其盐的方法
公开(公告)号：US5672755A
公开(公告)日：1997-09-30
申请号：US746575
申请日：1996-11-14
申请人： Ori Lerman , Michael Tennenbaum , Erez Gal , Joseph Kaspi
发明人： Ori Lerman , Michael Tennenbaum , Erez Gal , Joseph Kaspi
IPC分类号： C07C213/10 , C07C217/74 , C07C209/82
CPC分类号： C07C213/10 , C07C2101/14
摘要： The invention provides a process for the purification and isolation of (RR,SS)-2-dimethylaminomethyl-1-(3-methoxyphenyl)cyclohexanol from mixtures also containing the (RS,SR) isomer comprising reacting the above mixture in a solvent at elevated temperature under acidic conditions, whereby the (RS,SR) isomer is selectively converted to the (RR,SS) isomer, 1-(3-methoxyphenyl)-2-dimethylaminomethylcyclohex-6-ene, 1-(3-methoxyphenyl)-2-dimethyl-aminomethylcyclohex-1-ene or a mixture thereof, selectively precipitating the desired (RR,SS) isomer as an amine acid salt, and recrystallizing the purified product.
摘要翻译：本发明提供了从含有（RS，SR）异构体的混合物中纯化和分离（RR，SS）-2-二甲基氨基甲基-1-（3-甲氧基苯基）环己醇的方法，包括使上述混合物在溶剂中升高（RS，SR）异构体选择性转化为（RR，SS）异构体，1-（3-甲氧基苯基）-2-二甲基氨基甲基环己-6-烯，1-（3-甲氧基苯基）-2 - 二甲基 - 氨基甲基环己-1-烯或其混合物，选择性沉淀作为胺酸盐的所需的（RR，SS）异构体，并将纯化的产物重结晶。

6. 发明授权

US07208485B2 Crystalline forms of halobetasol propionate 失效
标题翻译：结晶形式的丙酸卤代倍他索
公开(公告)号：US07208485B2
公开(公告)日：2007-04-24
申请号：US10341690
申请日：2003-01-13
申请人： Itai Adin , Yuri Futerman , Ori Lerman , Alexander Weisman , Chaim Ashkenazi , Joseph Kaspi
发明人： Itai Adin , Yuri Futerman , Ori Lerman , Alexander Weisman , Chaim Ashkenazi , Joseph Kaspi
IPC分类号： A61K31/56 , C07J7/00
CPC分类号： A61K31/56 , C07J7/00
摘要： The present invention provides a crystalline halobetasol propionate selected from the group consisting of halobetasol propionate having crystalline Form I characterized by power X-ray diffraction peak positions and intensities as set forth in Table 1 herein, halobetasol propionate having crystalline Form II characterized by power X-ray diffraction peak positions and intensities as set forth in Table 2 herein, halobetasol propionate having crystalline Form III characterized by power X-ray diffraction peak positions and intensities as set forth in Table 3 herein, halobetasol propionate having crystalline Form IV characterized by power X-ray diffraction peak positions and intensities as set forth in Table 4 herein, halobetasol propionate having crystalline Form V characterized by power X-ray diffraction peak positions and intensities as set forth in Table 5 herein, and halobetasol propionate having crystalline Form VI characterized by power X-ray diffraction peak positions and intensities as set forth in Table 6 herein.
摘要翻译：本发明提供一种选自由具有结晶形式I的特征为结晶形式I的权利要求的表示于表1中的功能X射线衍射峰位置和强度的结晶形式的盐酸羟钴因子，如本文表2所示的X-射线衍射峰位置和强度，具有结晶形式III的盐酸羟考沙丹，其特征在于功能X射线衍射峰位置和强度，如表3所示，具有结晶形式IV的具有结晶形式IV的功能X- 如本文表4所示的X-射线衍射峰位置和强度，具有结晶形式V的具有由表X所示的功率X射线衍射峰位置和强度表征的结晶形式V的卤代双酚S和具有结晶形式VI的十六烷醇酯，其特征在于功率X 射线衍射峰位置和强度如本文表6所示。

7. 发明授权

US6100400A Process for the preparation of esters of [2-[4-[(4-chlorophenyl)phenylmethyl]-1-piperazinyl]-ethoxy]acetic acid 有权
标题翻译：制备[2- [4 - [（4-氯苯基）苯甲基] -1-哌嗪基] - 乙氧基]乙酸酯的方法
公开(公告)号：US6100400A
公开(公告)日：2000-08-08
申请号：US292318
申请日：1999-04-15
申请人： Ori Lerman , Erez Gal , Joseph Kaspi
发明人： Ori Lerman , Erez Gal , Joseph Kaspi
IPC分类号： C07D241/04 , C07D295/088 , C07D295/15
CPC分类号： C07D295/088
摘要： The invention provides a process for the preparation of esters [2-[4-[(4-chlorophenyl)phenylmethyl]-1-piperazinyl]ethoxy]acetic acid, of the formula (I) ##STR1## wherein X represents a halogen atom and R represents a lower alkyl group comprising reacting:(a) a compound of the formula (II) ##STR2## (b) a compound of the formula (III) ##STR3## and (c) a tertiary amine as a solvent and as an acid scavengerat a temperature of at least 100.degree. C., wherein X is a halogen atom, X' is selected from the group consisting of bromine and chlorine and R is a lower alkyl group.
摘要翻译：本发明提供了制备式（I）的酯[2- [4 - [（4-氯苯基）苯基甲基] -1-哌嗪基]乙氧基]乙酸的方法，其中X表示卤素原子，R表示包括使（a）式（II）的化合物（b）式（III）的化合物和（c）作为溶剂的叔胺和作为酸清除剂的化合物在至少100℃的温度下反应：其中X是卤素原子，X'选自溴和氯，R是低级烷基。

8. 发明申请

US20060241160A1 Zolmitriptan crystal forms 审中-公开
标题翻译：佐米曲坦水晶
公开(公告)号：US20060241160A1
公开(公告)日：2006-10-26
申请号：US11471367
申请日：2006-06-19
申请人： Reuven Izsak , Ori Lerman , Tamas Koltai , Judith Aronhime , Michael Pinchasov , Hagit Eisen-Nevo
发明人： Reuven Izsak , Ori Lerman , Tamas Koltai , Judith Aronhime , Michael Pinchasov , Hagit Eisen-Nevo
IPC分类号： A61K31/422 , C07D413/02
CPC分类号： C07D413/06
摘要： The invention encompasses novel crystalline forms of zolmitriptan herein defined as Form B, D, C, E, F, G, H, I, J, K, M, N, O, P, Q, R, S, or Amorphous and to methods of making thereof. The invention also encompasses methods of making zolmitriptan crystalline Form A.
摘要翻译：本发明包括本文定义为形式B，D，C，E，F，G，H，I，J，K，M，N，O，P，Q，R，S或无定形的佐米曲坦的新型结晶形式，制作方法。本发明还包括制备唑来曲坦结晶A型的方法。

9. 发明申请

US20060241158A1 Zolmitriptan crystal forms 审中-公开
公开(公告)号：US20060241158A1
公开(公告)日：2006-10-26
申请号：US11471364
申请日：2006-06-19
申请人： Reuven Izsak , Ori Lerman , Tamas Koltai , Judith Aronhime , Michael Pinchasov , Hagit Eisen-Nevo
发明人： Reuven Izsak , Ori Lerman , Tamas Koltai , Judith Aronhime , Michael Pinchasov , Hagit Eisen-Nevo
IPC分类号： A61K31/422 , C07D413/02
CPC分类号： C07D413/06
摘要： The invention encompasses novel crystalline forms of zolmitriptan herein defined as Form B, D, C, E, F, G, H, I, J, K, M, N, O, P, Q, R, S, or Amorphous and to methods of making thereof. The invention also encompasses methods of making zolmitriptan crystalline Form A.

10. 发明申请

US20060211751A1 Zolmitriptan crystal forms 审中-公开
公开(公告)号：US20060211751A1
公开(公告)日：2006-09-21
申请号：US11284773
申请日：2005-11-21
申请人： Reuven Izsak , Ori Lerman , Tamas Koltai , Judith Aronhime , Michael Pinchasov , Hagit Eisen-Nevo
发明人： Reuven Izsak , Ori Lerman , Tamas Koltai , Judith Aronhime , Michael Pinchasov , Hagit Eisen-Nevo
IPC分类号： A61K31/422 , C07D413/02
CPC分类号： C07D413/06
摘要： The invention encompasses novel crystalline forms of zolmitriptan herein defined as Form B, D, C, E, F, G, H, I, J, K, M, N, O, P, Q, R, S, or Amorphous and to methods of making thereof. The invention also encompasses methods of making zolmitriptan crystalline Form A.

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