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1. 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。

2. 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。

3. 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。

4. 发明授权

US06649796B2 Process for the preparation of acetamide derivatives 有权
公开(公告)号：US06649796B2
公开(公告)日：2003-11-18
申请号：US10112776
申请日：2002-04-02
申请人： Vladimir Naddaka , Naim Menashe , Jael Lexner , Shadi Saeed , Joseph Kaspi , Ori Lerman
发明人： Vladimir Naddaka , Naim Menashe , Jael Lexner , Shadi Saeed , Joseph Kaspi , Ori Lerman
IPC分类号： C07C32329
CPC分类号： C07C319/14 , C07C323/60
摘要： The invention provides a process for the preparation of diphenylmethylthioacetamide (I) as described in Scheme 4 comprising reacting of the isothiouronium salt or its corresponding base of the formula IV with an acetamide of the formula XCH2CONH2, wherein X represents a halogen, M represents an alkali metal and A represents an anion, in a protic medium at a temperature of less than 100° C.

5. 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％。

6. 发明授权

US06844440B2 Process for the preparation of donepezil 失效
标题翻译：多奈哌齐的制备方法
公开(公告)号：US06844440B2
公开(公告)日：2005-01-18
申请号：US10459662
申请日：2003-06-11
申请人： Ori Lerman , Joseph Kaspi , Oded Arad , Mohammed Alnabari , Yana Sery
发明人： Ori Lerman , Joseph Kaspi , Oded Arad , Mohammed Alnabari , Yana Sery
IPC分类号： A61P25/28 , C07D211/32 , C07D211/34 , C07D211/06
CPC分类号： C07D211/34 , C07D211/32 , Y02P20/55
摘要： The invention provides a process for the preparation of a compound of the formula 6 comprising the hydrolysis and decarboxylation of a compound of the formula 5 according to the reaction: wherein R and R2 independently a C1-C4 alkyl group or an aralkyl group.
摘要翻译：本发明提供了一种制备式6化合物的方法，其包括根据以下反应进行式5化合物的水解和脱羧作用：其中R和R 2独立地为C 1 -C 4烷基或芳烷基。

7. 发明授权

US5874620A Process for the purification of (RR-SS)-2-dimethylaminomethyl-1-(3-methoxyphenyl)cyclohexanol hydrochloride 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）环己醇盐酸盐的方法
公开(公告)号：US5874620A
公开(公告)日：1999-02-23
申请号：US911518
申请日：1997-08-14
申请人： Ori Lerman , Joseph Kaspi , Dov Brenner
发明人： Ori Lerman , Joseph Kaspi , Dov Brenner
IPC分类号： C07C213/10 , C07C217/74 , C07C209/88
CPC分类号： C07C213/10 , C07C2101/14
摘要： The invention provides a process for the separation of (RR,SS) 2-dimethylaminomethyl-1-(3-methoxyphenyl) cyclohexanol hydrochloride �(RR,SS)-Tramadol!, from a mixture consisting of (RR,SS) Tramadol and (RS,SR)-2-dimethylaminomethyl-1-(3-methoxyphenyl) cyclohexanol �(RS,SR)-Tramadol!, which process includes combining the mixture with an electrophilic reagent, the reagent selectively reacting with the hydroxyl group of (RS,SR)-Tramadol, leaving most of the (RR,SS) Tramadol intact, and precipitating the remaining, practically pure (RR,SS) Tramadol from the mixture.
摘要翻译：本发明提供了一种从（RR，SS）曲马多和（RR，SS） - 二甲氨基甲基-1-（3-甲氧基苯基）环己醇盐酸盐 RS，SR）-2-二甲基氨基甲基-1-（3-甲氧基苯基）环己醇[（RS，SR）-Tramadol]，该方法包括将该混合物与亲电试剂混合，该试剂选择性地与（RS， SR） - 曲马多，使大部分（RR，SS）曲马多完好无损，并从混合物中沉淀剩余的，实际上纯的（RR，SS）曲马多。

8. 发明授权

US5414129A Process for the purification of 2-[(dimethylamino)methyl]-1-(3-methoxyphenyl)cyclohexanol and its salts 失效
标题翻译：纯化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：US5414129A
公开(公告)日：1995-05-09
申请号：US117803
申请日：1993-09-08
申请人： Stephen Cherkez , Ori Lerman , Michael Tennenbaum , Hasalia Avner , Tamar Kunyevski
发明人： Stephen Cherkez , Ori Lerman , Michael Tennenbaum , Hasalia Avner , Tamar Kunyevski
IPC分类号： C07C213/10 , C07C209/84 , C07C209/86 , C07C209/88
CPC分类号： C07C213/10 , C07C2101/14
摘要： A process for the improved purification and separation of trans 2-[(dimethylamino)methyl]-1-(3-methoxyphenyl)cyclohexanol hydrochloride from a reaction mixture containing the trans isomer, the cis isomer and Grignard reaction side products, comprising combining the mixture with a solution of hydrochloric acid in a low molecular weight alcohol or with gaseous hydrogen chloride in the presence of an organic solvent selected from medium molecular weight alcohols, ketones, esters and ethers or aromatic ethers, to effect the selective precipitation of trans 2-[(dimethylamino)methyl]-1-(3-methoxyphenyl)cyclohexanol hydrochloride.
摘要翻译：从含有反式异构体，顺式异构体和格利雅反应副产物的反应混合物中改进反式-2 - [（二甲基氨基）甲基] -1-（3-甲氧基苯基）环己醇盐酸盐的纯化和分离的方法，包括将混合物在选自中等分子量的醇，酮，酯和醚或芳族醚的有机溶剂的存在下，用盐酸在低分子量醇或气体氯化氢中的溶液进行反式2- [ （二甲基氨基）甲基] -1-（3-甲氧基苯基）环己醇盐酸盐。

9. 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。

10. 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。

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