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1. 发明授权

US08420806B2 Process for the crystallisation of cefadroxil monohydrate 有权
标题翻译：头孢羟氨苄一水合物结晶方法
公开(公告)号：US08420806B2
公开(公告)日：2013-04-16
申请号：US12300046
申请日：2007-05-11
申请人： Carlos Enrique Lenhard , Harold Monro Moody , Theodorus Johannes Godfried Maria Van Dooren
发明人： Carlos Enrique Lenhard , Harold Monro Moody , Theodorus Johannes Godfried Maria Van Dooren
IPC分类号： C07D501/22 , A61K31/546
CPC分类号： C07D501/20 , C07D501/12 , C07D501/22
摘要： The present invention relates to a process for the preparation of cefadroxil in crystal form, comprising a) adding an aqueous solution of cefadroxil to a crystallization vessel and a titrant to keep a pH in the crystallization vessel of between 7 to 9; and b) lowering the pH in the crystallization vessel to a value of between 5 and 6.5 to obtain a suspension of the β-lactam compound in crystal form. The invention further relates to cefadroxil in crystal form obtainable by the process according to the present invention. The invention also relates to cefadroxil in crystal form with a CIE b value of below 12 when stored at a temperature of 25° C. for at least 1 month.
摘要翻译：本发明涉及一种晶体形式的头孢羟氨苄的制备方法，其包括：a）向结晶容器中加入头孢羟氨苄水溶液，滴定剂将结晶容器中的pH值保持在7-9之间; 和b）将结晶容器中的pH降低至5至6.5的值，以获得晶体形式的β-内酰胺化合物的悬浮液。本发明还涉及通过本发明的方法获得的晶体形式的头孢羟氨苄。本发明还涉及当在25℃的温度下储存至少1个月时，CIE b值低于12的晶体形式的头孢羟氨苄。

2. 发明申请

US20100010213A1 PROCESS FOR THE CRYSTALLISATION OF CEFADROXIL 有权
标题翻译：氯吡格雷的结晶过程
公开(公告)号：US20100010213A1
公开(公告)日：2010-01-14
申请号：US12300046
申请日：2007-05-11
申请人： Carlos Enrique Lenhard , Harold Monro Moody , Theodorus Johannes Godfried Maria Van Dooren
发明人： Carlos Enrique Lenhard , Harold Monro Moody , Theodorus Johannes Godfried Maria Van Dooren
IPC分类号： C07D501/02
CPC分类号： C07D501/20 , C07D501/12 , C07D501/22
摘要： The present invention relates to a process for the preparation of cefadroxil in crystal form, comprising a) adding an aqueous solution of cefadroxil to a crystallisation vessel and a titrant to keep a pH in the crystallisation vessel of between 7 to 9; and b) lowering the pH in the crystallisation vessel to a value of between 5 and 6.5 to obtain a suspension of the β-lactam compound in crystal form. The invention further relates to cefadroxil in crystal form obtainable by the process according to the present invention. The invention also relates to cefadroxil in crystal form with a CIE b value of below 12 when stored at a temperature of 25° C. for at least 1 month.
摘要翻译：本发明涉及一种制备晶体形式的头孢羟氨苄的方法，其包括：a）将Cefadroxil水溶液加到结晶容器中，并将滴定剂保持在结晶容器中的pH在7至9之间; 和b）将结晶容器中的pH降低至5至6.5之间的值，以获得晶体形式的β-内酰胺化合物的悬浮液。本发明还涉及通过本发明的方法获得的晶体形式的头孢羟氨苄。本发明还涉及当在25℃的温度下储存至少1个月时，CIE b值低于12的晶体形式的头孢羟氨苄。

3. 发明申请

US20110104748A1 PROCESS FOR THE PREPARATION OF BETA-LACTAM COMPOUNDS 有权
标题翻译：制备BETA-LACTAM化合物的方法
公开(公告)号：US20110104748A1
公开(公告)日：2011-05-05
申请号：US12528695
申请日：2008-03-10
申请人： Thomas Van Der Does , Harold Monro Moody , Theodorus Johannes Godfried Maria Van Dooren
发明人： Thomas Van Der Does , Harold Monro Moody , Theodorus Johannes Godfried Maria Van Dooren
IPC分类号： C12P37/00 , C12P35/00 , C07C229/28
CPC分类号： C12P35/04 , C07D499/21 , C07D501/22 , C12P35/06 , C12P37/04
摘要： The present invention describes a process for the synthesis of a semi-synthetic β-lactam compound from a nucleus and a side chain selected from the group consisting of D-phenylglycine and D-dihydro-phenylglycine in the form of a side chain ester and an enzyme catalyzing the coupling of the side chain ester to the nucleus characterized in that the side chain ester is not isolated as a solid intermediate.
摘要翻译：本发明描述了一种从侧链中合成半合成β-内酰胺化合物的方法，所述核和侧链选自D-苯基甘氨酸和D-二氢 - 苯基甘氨酸，其为侧链酯形式，催化侧链酯与核的偶联的酶，其特征在于侧链酯不作为固体中间体分离。

4. 发明申请

US20100311113A1 CHEMO-ENZYMATIC PEPTIDE SYNTHESIS VIA C-TERMINAL ESTER INTERCONVERSION 有权
标题翻译：化学合成肽通过C末端反应器合成
公开(公告)号：US20100311113A1
公开(公告)日：2010-12-09
申请号：US12682653
申请日：2008-10-09
申请人： Peter Jan Leonard Mario Quaedflieg , Timo Nuijens , Claudia Cusan , Harold Monro Moody , Theodorus Johannes Godfried Maria Van Dooren
发明人： Peter Jan Leonard Mario Quaedflieg , Timo Nuijens , Claudia Cusan , Harold Monro Moody , Theodorus Johannes Godfried Maria Van Dooren
IPC分类号： C12P21/00
CPC分类号： C12P7/62 , C12P13/02 , C12P13/04 , C12P13/06 , C12P13/08 , C12P13/12 , C12P13/222 , C12P21/02
摘要： The invention relates to a method for preparing an optionally N-protected amino acid C-terminal ester or an optionally N-protected peptide C-terminal ester, comprising transesterifying the C-terminal t-alkyl ester of the amino acid or the C-terminal t-alkyl ester of the peptide with an alcohol (other than the t-alcohol corresponding to the t-alkyl group of the ester) in the presence of a hydrolytic enzyme (E.C. 3).The invention further relates to a method for preparing a peptide comprising coupling an activated, N-protected, amino acid C-terminal ester or an optionally N-protected peptide C-terminal ester with an optionally C-terminal protected amino acid or an optionally C-terminal protected peptide via a peptide bond, in the presence of an enzyme catalysing peptidic bond formation.
摘要翻译：本发明涉及一种制备任选N-保护的氨基酸C-末端酯或任选N-保护的肽C-末端酯的方法，该方法包括将氨基酸或C末端的C末端叔烷基酯酯交换在水解酶（EC 3）的存在下，该肽与醇（除了对应于酯的叔烷基的叔醇以外）的叔烷基酯。本发明还涉及一种制备肽的方法，其包括将活化的N-保护的氨基酸C-末端酯或任选N-保护的肽C末端酯与任选C末端保护的氨基酸或任选的C 在催化肽键形成的酶存在下通过肽键进行末端保护的肽。

5. 发明授权

US08450084B2 Chemo-enzymatic peptide synthesis via C-terminal ester interconversion 有权
标题翻译：通过C端酯相互转化的化学酶肽合成
公开(公告)号：US08450084B2
公开(公告)日：2013-05-28
申请号：US12682653
申请日：2008-10-09
申请人： Peter Jan Leonard Mario Quaedflieg , Timo Nuijens , Claudia Cusan , Harold Monro Moody , Theodorus Johannes Godfried Maria Van Dooren
发明人： Peter Jan Leonard Mario Quaedflieg , Timo Nuijens , Claudia Cusan , Harold Monro Moody , Theodorus Johannes Godfried Maria Van Dooren
IPC分类号： C12P21/06 , C12P7/62
CPC分类号： C12P7/62 , C12P13/02 , C12P13/04 , C12P13/06 , C12P13/08 , C12P13/12 , C12P13/222 , C12P21/02
摘要： The invention relates to a method for preparing an optionally N-protected amino acid C-terminal ester or an optionally N-protected peptide C-terminal ester, comprising transesterifying the C-terminal t-alkyl ester of the amino acid or the C-terminal t-alkyl ester of the peptide with an alcohol (other than the t-alcohol corresponding to the t-alkyl group of the ester) in the presence of a hydrolytic enzyme (E.C. 3).The invention further relates to a method for preparing a peptide comprising coupling an activated, N-protected, amino acid C-terminal ester or an optionally N-protected peptide C-terminal ester with an optionally C-terminal protected amino acid or an optionally C-terminal protected peptide via a peptide bond, in the presence of an enzyme catalysing peptidic bond formation.
摘要翻译：本发明涉及一种制备任选N-保护的氨基酸C-末端酯或任选N-保护的肽C-末端酯的方法，该方法包括将氨基酸或C末端的C末端叔烷基酯酯交换在水解酶（EC 3）的存在下，该肽与醇（除了对应于酯的叔烷基的叔醇以外）的叔烷基酯。本发明还涉及一种制备肽的方法，其包括将活化的N-保护的氨基酸C-末端酯或任选N-保护的肽C末端酯与任选C末端保护的氨基酸或任选的C 在催化肽键形成的酶存在下通过肽键进行末端保护的肽。

6. 发明授权

US08071330B2 Process for the synthesis of cefaclor 有权
标题翻译：头孢克洛合成方法
公开(公告)号：US08071330B2
公开(公告)日：2011-12-06
申请号：US11794119
申请日：2005-12-23
申请人： Harold Monro Moody , Theodorus Johannes Godfried Maria Van Dooren
发明人： Harold Monro Moody , Theodorus Johannes Godfried Maria Van Dooren
IPC分类号： C12P35/04
CPC分类号： C12P35/04 , C07D501/58 , C12P35/00
摘要： The present invention relates to a process for the synthesis of cefaclor, which process comprises reacting 7-amino-3-chloro cephalosporanic acid (7-ACCA) with D-phenylglycine in activated form (PGa) in the presence of an enzyme in a reaction mixture to form cefaclor, wherein at least part of 7-ACCA and/or PGa are added to the reaction mixture during the course of the reaction. The invention also relates to an aqueous mixture comprising an amount of cefaclor of >10 (w/w) %, an amount of 7-amino-3-chloro cephalosporanic acid of
摘要翻译：本发明涉及一种头孢克洛的合成方法，该方法包括使7-氨基-3-氯头孢菌酸（7-ACCA）与活性形式的D-苯基甘氨酸（PGa）在酶的存在下反应混合物以形成头孢克洛，其中在反应过程中将7-ACCA和/或PGa的至少一部分加入到反应混合物中。本发明还涉及包含一定量的头孢克洛> 10（w / w）％，7-氨基-3-氯头孢菌酸的量<2（w / w）％和D量（w / w）％的苯基甘氨酸和从该水性混合物中回收头孢克洛的方法。本发明还涉及在400nm（A400）下的吸光度小于0.250的晶体形式的头孢克洛。

7. 发明授权

US08497088B2 Process for the preparation of beta-lactam compounds 有权
标题翻译：制备β-内酰胺化合物的方法
公开(公告)号：US08497088B2
公开(公告)日：2013-07-30
申请号：US12528695
申请日：2008-03-10
申请人： Thomas Van Der Does , Harold Monro Moody , Theodorus Johannes Godfried Maria Van Dooren
发明人： Thomas Van Der Does , Harold Monro Moody , Theodorus Johannes Godfried Maria Van Dooren
IPC分类号： C12P1/00
CPC分类号： C12P35/04 , C07D499/21 , C07D501/22 , C12P35/06 , C12P37/04
摘要： The present invention describes a process for the synthesis of a semi-synthetic β-lactam compound from a nucleus and a side chain selected from the group consisting of D-phenylglycine and D-dihydro-phenylglycine in the form of a side chain ester and an enzyme catalyzing the coupling of the side chain ester to the nucleus characterized in that the side chain ester is not isolated as a solid intermediate.
摘要翻译：本发明描述了从细胞核和侧链合成半合成β-内酰胺化合物的方法，该方法选自D-苯基甘氨酸和D-二氢 - 苯基甘氨酸，其为侧链酯和催化侧链酯与核的偶联的酶，其特征在于侧链酯不作为固体中间体分离。

8. 发明授权

US07588913B2 Process for the preparation of cephradine 有权
标题翻译：制备头孢拉定的方法
公开(公告)号：US07588913B2
公开(公告)日：2009-09-15
申请号：US10562345
申请日：2004-07-01
申请人： Dennis Heemskerk , Anja Gerarda Margaretha Hogenboom , Carlos Enrique Lenhardt , Harold Monro Moody , Theodorus Johannes Godfried Maria Van Dooren
发明人： Dennis Heemskerk , Anja Gerarda Margaretha Hogenboom , Carlos Enrique Lenhardt , Harold Monro Moody , Theodorus Johannes Godfried Maria Van Dooren
IPC分类号： C12P35/04 , C07D501/22
CPC分类号： C07D501/00 , C12P35/04
摘要： The present invention describes a process for preparing cephradine, said process comprising reacting 7-aminodesacetoxy cephalosporanic acid (7-ADCA) with D-dihydrophenylglycine in activated form (DHa) in the presence of an enzyme in a reaction mixture to form cephradine, resulting in a conversion of 7-ADCA into cephradine of at least 70%, wherein the concentration D-dihydrophenylglycine (DH) in the reaction mixture is below 2 wt.%, wherein the conversion of 7-ADCA into cephradine & equals; (nCEF/n7-ADCA)*100%, wherein nCEF=quantity of cephradine formed (in mole); and n7-ADCA=total quantity of 7-ADCA added to reaction mixture (in mole). The invention also describes a process for the preparation of cephradine hydrate characterised in that the process comprises: —reacting 7-amino acid desacetoxy cephalosporanic acid (7-ADCA) with DHa in the presence of an enzyme in a reaction mixture to form cephradine; —preparing an aqueous solution comprising at least part of the cephradine; and crystallising the cephradine from said aqueous solution. The invention further describes cephradine hydrate obtainable by a process according to invention. The invention also describes cephradine hydrate with an absorbance at 450 nm of below 0.050.
摘要翻译：本发明描述了一种制备头孢拉定的方法，所述方法包括使7-氨基二乙酰氧基头孢菌酸（7-ADCA）与活化形式的二氢苯基甘氨酸（DHa）在酶的存在下在反应混合物中反应形成头孢拉定，得到将7-ADCA转化为至少70％的头孢拉定，其中反应混合物中D-二氢苯基甘氨酸（DH）的浓度低于2重量％，其中7-ADCA转化成头孢拉定等于; （nCEF / n7-ADCA）* 100％，其中nCEF =形成的头孢拉定量（以摩尔计）; 和n7-ADCA =加入到反应混合物中的7-ADCA的总量（以摩尔计）。本发明还描述了一种制备头孢拉定水合物的方法，其特征在于该方法包括：在反应混合物中，在酶的存在下，用7-氨基酸脱乙酰氧基头孢菌酸（7-ADCA）与DHa反应形成头孢拉定; - 制备包含至少一部分头孢拉定的水溶液; 并从所述水溶液中结晶头孢拉定。本发明还描述了通过根据本发明的方法获得的头孢拉定水合物。本发明还描述了在450nm处的吸光度低于0.050的头孢拉定水合物。

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