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1. 发明授权

US5440046A Substituted imidazoles 失效
标题翻译：取代的咪唑
公开(公告)号：US5440046A
公开(公告)日：1995-08-08
申请号：US250491
申请日：1994-05-27
申请人： Adalbert Wagner , Rainer Henning , Hermann Gerhards , Bernward Scholkens , Jean-Paul Vevert , Jean-Claude Caille
发明人： Adalbert Wagner , Rainer Henning , Hermann Gerhards , Bernward Scholkens , Jean-Paul Vevert , Jean-Claude Caille
IPC分类号： A61K31/415 , A61K31/38 , A61K31/40 , A61K31/41 , A61K31/4155 , A61K31/4164 , A61K31/423 , A61K31/437 , A61K31/44 , A61K31/443 , A61K31/4433 , A61K31/495 , A61K31/505 , A61K31/519 , A61P9/12 , A61P29/00 , A61P43/00 , C07D233/64 , C07D233/84 , C07D233/90 , C07D403/06 , C07D405/06 , C07D409/06 , C07D409/14 , C07D413/06 , C07D471/04 , C07D487/04 , C07D401/04 , C07D405/04 , C07D409/04
CPC分类号： C07D403/06 , C07D405/06 , C07D409/06 , C07D409/14 , C07D413/06 , C07D471/04 , C07D487/04
摘要： The invention relates to compounds of the formula ##STR1## in which X, Y and Z are identical or different and are N or CR.sup.2, L is an alkylene radical, q is 0 or 1, and A is the radical of a fused heterobicyclic compound. The invention furthermore relates to a process for preparing the said compounds, agents containing these, and the use thereof for angiotensin II receptors.
摘要翻译：本发明涉及其中X，Y和Z相同或不同且为N或CR2的式“IMAGE”的化合物，L为亚烷基，q为0或1，A为稠合杂双环化合物的基团。本发明还涉及制备所述化合物的方法，含有它们的药剂及其用于血管紧张素II受体的方法。

2. 发明授权

US5350751A Substituted imidazoles, pharmaceutical compositions containing these, and the use thereof as antagonists of angiotensin II receptors for the treatment of high blood pressure 失效
标题翻译：取代的咪唑，含有这些的药物组合物，以及作为血管紧张素II受体拮抗剂用于治疗高血压的用途
公开(公告)号：US5350751A
公开(公告)日：1994-09-27
申请号：US679233
申请日：1991-04-02
申请人： Adalbert Wagner , Rainer Henning , Hermann Gerhards , Bernward Scholkens , Jean-Paul Vevert , Jean-Claude Caille
发明人： Adalbert Wagner , Rainer Henning , Hermann Gerhards , Bernward Scholkens , Jean-Paul Vevert , Jean-Claude Caille
IPC分类号： A61K31/415 , A61K31/38 , A61K31/40 , A61K31/41 , A61K31/4155 , A61K31/4164 , A61K31/423 , A61K31/437 , A61K31/44 , A61K31/443 , A61K31/4433 , A61K31/495 , A61K31/505 , A61K31/519 , A61P9/12 , A61P29/00 , A61P43/00 , C07D233/64 , C07D233/84 , C07D233/90 , C07D403/06 , C07D405/06 , C07D409/06 , C07D409/14 , C07D413/06 , C07D471/04 , C07D487/04 , C07D233/57 , C07D401/02 , C07D403/02 , C07D405/02 , C07D407/02 , A61K311/415
CPC分类号： C07D403/06 , C07D405/06 , C07D409/06 , C07D409/14 , C07D413/06 , C07D471/04 , C07D487/04
摘要： The invention relates to compounds of the formula I ##STR1## in which X, Y and Z are identical or different and are N or CR.sup.2, R.sup.1 and R.sup.2 are as defined in the description, L is an alkylene radical, q is 0 or 1, and A is the radical of a fused heterobicyclic compound. The invention furthermore relates to a process for preparing the said compounds, agents containing these, and the use thereof in the treatment of high blood pressure.
摘要翻译：本发明涉及式I（I）的化合物，其中X，Y和Z相同或不同，为N或CR2，R1和R2如说明书中所定义，L为亚烷基，q为 0或1，A是稠合杂双环化合物的基团。本发明还涉及制备所述化合物的方法，含有这些化合物的药剂及其在治疗高血压中的用途。

3. 发明授权

US5474996A Pyrimidine derivatives 失效
标题翻译：嘧啶衍生物
公开(公告)号：US5474996A
公开(公告)日：1995-12-12
申请号：US888750
申请日：1992-05-22
申请人： Jean-Claude Caille , Stanislas Didierlaurent , Jean-Paul Vevert
发明人： Jean-Claude Caille , Stanislas Didierlaurent , Jean-Paul Vevert
IPC分类号： A61K31/505 , A61K31/506 , A61P9/12 , A61P43/00 , C07D239/26 , C07D239/30 , C07D239/34 , C07D239/54 , C07D401/04 , C07D403/04 , C07D403/10 , C07D405/04 , C07D417/10
CPC分类号： C07D239/26 , C07D239/34 , C07D239/54 , C07D403/10 , C07D417/10
摘要： Novel pyrimidine derivatives of the formula ##STR1## represents: either a group: ##STR2## or a group: ##STR3## having angiotensin II inhibiting activity.
摘要翻译：新颖的式（I）的嘧啶衍生物，其中：表示：具有血管紧张素II抑制活性的组：或组：。

4. 发明申请

US20070225516A1 Process for the diastereoselective alkylation of an ether oxime of the compound nopinone and novel intermediates for the synthesis of diastereospecific 2-amino-nopinone derivatives substituted on carbon 3 失效
标题翻译：化合物胭脂膦的醚肟的非对映选择性烷基化方法和用于合成在碳上取代的非对映异构2-氨基n酮衍生物的新中间体
公开(公告)号：US20070225516A1
公开(公告)日：2007-09-27
申请号：US11484991
申请日：2006-07-12
申请人： Jean-Claude Caille , Marc Mauduit
发明人： Jean-Claude Caille , Marc Mauduit
IPC分类号： C07F7/04 , C07C215/42
CPC分类号： C07C251/44 , C07B2200/07 , C07C215/42 , C07C2602/42
摘要： The invention provides the diastereoselective alkylation of optically active nopinone to form the compound of formula (I) according to scheme A below: in which: R is a C5-15 alkyl group; R1 is especially a C1-15 alkyl, C2-15 alkenyl or C2-15 alkynyl group or a C5-15 aryl, each group optionally being substituted; and X is a halogen atom; and the configuration of the compound of formula (I) is either (E) or (Z) or a mixture of the two. The compound of formula (I) is a valuable synthetic intermediate.
摘要翻译：本发明提供了光学活性硫蛋白酮的非对映选择性烷基化，以形成根据方案A的式（I）化合物：其中：R是C 5-15烷基; R1特别是C 1-15烷基，C 2-15链烯基或C 2-15-15炔基或C 5 -15个芳基，每个基团任选被取代; X为卤素原子; 式（I）化合物的构型是（E）或（Z）或两者的混合物。式（I）化合物是有价值的合成中间体。

5. 发明授权

US08198054B2 Method for the chemo-selective enzymatic hydrolysis if a diester compound for preparing a monoester monoacid compound 有权
标题翻译：用于制备单酯一酸化合物的二酯化合物的化学选择性酶水解的方法
公开(公告)号：US08198054B2
公开(公告)日：2012-06-12
申请号：US12523602
申请日：2008-01-22
申请人： Alain Burgos , Jean-Claude Caille , Michelle Lorraine-Gradley
发明人： Alain Burgos , Jean-Claude Caille , Michelle Lorraine-Gradley
IPC分类号： C12P7/40
CPC分类号： C12P7/62
摘要： This disclosure relates to the synthesis of the compound of formula (I) according to Scheme A below: in which R1, R2 and R3, which may be identical or different, represent, individually and independently, an alkyl group, characterized by an enzymatic hydrolysis reaction that involves placing the compound of formula (II) in contact with an enzyme that performs a chemoselective hydrolysis of only one of the two ester functions of the compound of formula (II) to obtain the compound of formula (I).
摘要翻译：本公开涉及根据下文方案A的式（I）化合物的合成：其中可以相同或不同的R 1，R 2和R 3各自独立地表示烷基，其特征在于酶水解涉及将式（II）的化合物与仅进行式（II）化合物的两种酯官能团的化学选择性水解的酶接触以获得式（I）的化合物的反应。

6. 发明申请

US20100068770A1 METHOD FOR THE CHEMO-SELECTIVE ENZYMATIC HYDROLYSIS IF A DIESTER COMPOUND FOR PREPARING A MONOESTER MONOACID COMPOUND 有权
标题翻译：如果用于制备单体单体化合物的DIESTER化合物的选择性酶水解的方法
公开(公告)号：US20100068770A1
公开(公告)日：2010-03-18
申请号：US12523602
申请日：2008-01-22
申请人： Alain Burgos , Jean-Claude Caille , Michelle Lorraine Gradley
发明人： Alain Burgos , Jean-Claude Caille , Michelle Lorraine Gradley
IPC分类号： C12P17/12 , C12P7/62
CPC分类号： C12P7/62
摘要： The invention relates to a synthesis process.This process relates to the synthesis of the compound of formula (I) according to Scheme A below: in which R1, R2 and R3, which may be identical or different, represent, individually and independently, an alkyl group, characterized by an enzymatic hydrolysis reaction that involves placing the compound of formula (II) in contact with an enzyme that performs a chemoselective hydrolysis of only one of the two ester functions of the compound of formula (II) to obtain the compound of formula (I).The invention allows the industrial preparation of the intermediate of formula (I), which may be used for the preparation of the pharmaceutical active principle repaglinide.
摘要翻译：本发明涉及一种合成方法。该方法涉及根据下文方案A的式（I）化合物的合成：其中可以相同或不同的R 1，R 2和R 3各自独立地表示烷基，其特征在于酶水解涉及将式（II）的化合物与仅进行式（II）化合物的两种酯官能团的化学选择性水解的酶接触以获得式（I）的化合物的反应。本发明允许工业制备式（I）的中间体，其可用于制备药物活性成分瑞格列奈。

7. 发明授权

US07390926B2 Process for the diastereoselective alkylation of an ether oxime of the compound nopinone and novel intermediates for the synthesis of diastereospecific 2-amino-nopinone derivatives substituted on carbon 3 失效
标题翻译：化合物胭脂膦的醚肟的非对映选择性烷基化方法和用于合成在碳上取代的非对映异构2-氨基n酮衍生物的新中间体
公开(公告)号：US07390926B2
公开(公告)日：2008-06-24
申请号：US11484991
申请日：2006-07-12
申请人： Jean-Claude Caille , Marc Mauduit
发明人： Jean-Claude Caille , Marc Mauduit
IPC分类号： C07C249/00 , C07C251/00 , C07C259/00 , C07C291/00
CPC分类号： C07C251/44 , C07B2200/07 , C07C215/42 , C07C2602/42
摘要： The invention provides the diastereoselective alkylation of optically active nopinone to form the compound of formula (I) according to scheme A below: in which: —R is a C5-15 alkyl group; —R1 is especially a C1-15 alkyl, C2-15 alkenyl or C2-15 alkynyl group or a C5-15 aryl, each group optionally being substituted; and —X is a halogen atom; and the configuration of the compound of formula (I) is either (E) or (Z) or a mixture of the two. The compound of formula (I) is a valuable synthetic intermediate.
摘要翻译：本发明提供光学活性硫蛋白酮的非对映选择性烷基化，以形成根据方案A的式（I）化合物：其中：-R为C 5-15烷基; -R1特别是C 1-15烷基，C 2-15-15烯基或C 2-15-15炔基或C 1 -C 6烷基， 5-15个芳基，每个基团任选被取代; 且-X为卤素原子; 式（I）化合物的构型是（E）或（Z）或两者的混合物。式（I）化合物是有价值的合成中间体。

8. 发明授权

US06300106B1 Method of preparing 3-[2-{(Methylsulfonyl)oxy}-ethoxy ]-4-(triphenylmethoxy)-1-butanol, methane sulfonate 失效
标题翻译：制备3- [2 - {（甲基磺酰基）氧基} - 乙氧基] -4-（三苯甲氧基）-1-丁醇甲磺酸盐的方法
公开(公告)号：US06300106B1
公开(公告)日：2001-10-09
申请号：US09718711
申请日：2000-11-22
申请人： Jean-Claude Caille
发明人： Jean-Claude Caille
IPC分类号： C12P1706
CPC分类号： C12P41/001 , C07C303/28 , C07D309/24 , C12P11/00 , C07C309/66
摘要： A method of producing (S)-3-[2-{(methylsulfonyl)oxy}ethoxy]-4-(triphenylmethoxy)-1-butanol methane sulfonate using 1,3-butadiene and a ketoethanal to form an intermediate racemic mixture. The racemic mixture is resolved to remove one isomer from the reaction product mixture. Following resolution, the following steps are performed: reduce the isomer to an alcohol, react the alcohol with triphenylmethyl chloride, ozonalyze the resulting reaction product, reduce the ozonalyzed product to yield a diol and react the diol with a methane sulfonyl compound to form (S)-3-[2-{(methylsulfonyl)oxy}ethoxy]-4-(triphenylmethoxy)-1-butanol methane sulfonate. Alternatively, the racemic mixture may first be reduced and the resulting racemic alcohol mixture is resolved to isolate one isomer of the alcohol and the remaining process steps are followed.
摘要翻译：使用1,3-丁二烯和酮代乙醇制备（S）-3- [2 - {（甲基磺酰基）氧基}乙氧基] -4-（三苯甲氧基）-1-丁醇甲磺酸盐以形成中间体外消旋混合物的方法。拆分外消旋混合物以从反应产物混合物中除去一种异构体。进行以下步骤：将异构体还原成醇，将其与三苯基甲基氯反应，对所得反应产物进行臭氧分解，减少臭氧分解产物，得到二醇并使二醇与甲磺酰化合物反应形成（S ）-3- [2 - {（甲基磺酰基）氧基}乙氧基] -4-（三苯甲氧基）-1-丁醇甲磺酸盐。或者，可以首先降低外消旋混合物，并将所得外消旋醇混合物溶解以分离醇的一种异构体，并遵循剩余的方法步骤。

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