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41. 发明公开

EP1456393A1 CYCLISATION PROCESS FOR THE PREPARATION OF C-2 BETA-LACTAM COMPOUNDS 审中-公开
标题翻译：环化经取代C-2的β-内酰胺连接的生产
公开(公告)号：EP1456393A1
公开(公告)日：2004-09-15
申请号：EP02804967.4
申请日：2002-12-19
申请人： ISIS INNOVATION LIMITED
发明人： SCHOFIELD, Christopher Joseph , HEWITSON, Kirsty Sarah , SLEEMAN, Mark Christopher
IPC分类号： C12P17/10 , C07D205/08 , C07D205/12
CPC分类号： C12P17/10 , C07D205/08 , C07D477/04 , C07D503/00
摘要： A process for the preparation of a substituted C-2 β-lactam comprises incubating a 2-substituted 3-aminocarboxylic acid with a β-lactam synthetase under conditions such that the 2-substituted 3-aminocarboxylic acid is cyclised to produce a substituted C-2 β-lactam. The process can be used to produce an antibiotic or β-lactamase inhibitor.

42. 发明公开

EP1346981A1 PROCESS FOR SYNTHESIZING $g(b)-LACTAM 有权
标题翻译： VERFAHREN ZUR SYNTHESE VON？-LACTAMEN
公开(公告)号：EP1346981A1
公开(公告)日：2003-09-24
申请号：EP01912138.3
申请日：2001-03-07
申请人： National Institute of Advanced Industrial Science and Technology
发明人： HATAKEDA, Kiyotaka , SATO, Osamu , KANAKUBO, Mitsuhiro , IKUSHIMA, Yutaka , TORII, Kazuo
IPC分类号： C07D201/08 , C07D205/08
CPC分类号： C07D201/08 , Y02P20/582
摘要： It is an object of the present invention to provide a method for synthesizing β-lactams and a method for manufacturing β-lactams in water of high-temperature and under high-pressure, and the present invention relates to a β-lactam synthesis method which is characterized in that β-lactams are synthesized by reacting β-amino acids in water at high-temperature and under high-pressure, this method being further characterized in that β-lactams are synthesized at a high speed by cyclizing β-amino acids in water at high-temperature and under high-pressure in which the temperature range is 200°C or higher and the pressure range is 10 MPa or greater, and the present invention also relates to a method for manufacturing β-lactams which is characterized in that β-lactams are synthesized by reacting β-amino acids in water at high-temperature and under high-pressure, and are then separated and purified using a column separation medium.
摘要翻译：本发明的目的是提供一种合成β-内酰胺的方法和在高温和高压水中制备β-内酰胺的方法，本发明涉及β-内酰胺合成方法其特征在于通过β-氨基酸在高温和高压下在水中反应来合成β-内酰胺，该方法的进一步特征在于通过使β-氨基酸在高温和高压下环化β-氨基酸来合成β-内酰胺在温度范围为200℃以上且压力范围为10MPa以上的高温高压下的水，本发明还涉及β-内酰胺的制造方法，其特征在于， β-内酰胺通过在高温和高压下在水中使β-氨基酸反应合成，然后使用柱分离介质分离和纯化。

43. 发明授权

EP0971889B1 PROCESS FOR SYNTHESIZING CARBAPENEM INTERMEDIATES 失效
标题翻译：于制备碳青霉烯类抗生素的中间体
公开(公告)号：EP0971889B1
公开(公告)日：2003-08-13
申请号：EP98902597.8
申请日：1998-01-16
申请人： MERCK & CO., INC.
发明人： YASUDA, Nobuyoshi , YANG, Chunhua
IPC分类号： C07D205/08 , C07F7/08 , C07F7/18
CPC分类号： C07F7/1892 , C07D205/08 , C07F7/186 , Y02P20/55

44. 发明公开

EP1316610A1 Preparation comprising an enzyme for asymmetrical hydrolysis of N-substituted C3-C4 cyclic imino-2-carboxylic acid ester and method of using the same 有权
标题翻译：它包含N-取代的C3-C4环亚胺-2-羧酸酯和不对称水解的酶的化合物，它们的使用
公开(公告)号：EP1316610A1
公开(公告)日：2003-06-04
申请号：EP02256033.8
申请日：2002-08-30
申请人： Sumitomo Chemical Company, Limited
发明人： Kawabe, Tomoyasu , Kamitamari, Masashi
IPC分类号： C12N15/55 , C12N11/08 , C12N9/18 , C07D205/08
CPC分类号： C12N9/18 , C07D205/04
摘要： There is disclosed an enzyme preparation comprising: (i) a styrene-divinylbenzene copolymer having fine pores with an average radius of 200 - 500Å, and (ii) an enzyme capable of asymmetrically hydrolyzing N-substituted C3-C4 cyclic imino-2-carboxylic acid ester to preferentially produce an (S)-N-substituted C3-C4 cyclic imino-2-carboxylic acid, wherein said enzyme comprises an amino acid sequence as set forth in SEQ ID NO: 1 or the like.
摘要翻译：有在游离缺失的酶制剂，其包括光盘：（i）具有细孔上的200至500埃平均半径的苯乙烯 - 二乙烯基苯共聚物，和（ii）酶能够不对称水解的N- substituiertem C3-C4环亚胺-2- 羧酸酯以优先产生于（S）-N-取代的C3-C4环亚胺-2-羧酸，worin所述酶在氨基酸序列包含如SEQ ID NO：1中列出或类似物。

45. 发明授权

EP1023265B1 AZETIDINONE DERIVATIVES FOR THE TREATMENT OF HCMV INFECTIONS 有权
标题翻译：用于治疗HCMV炎症氮杂环丁酮衍生物
公开(公告)号：EP1023265B1
公开(公告)日：2003-01-15
申请号：EP98947257.6
申请日：1998-10-06
申请人： BOEHRINGER INGELHEIM (CANADA) LTD.
发明人： YOAKIM, Christiane , CHABOT, Catherine , DEZIEL, Robert , KAWAI, Stephen , OGILVIE, Willian, W. , O'MEARA, Jeffrey
IPC分类号： C07D205/08 , A61K31/395
CPC分类号： C07D205/08 , C07D403/12
摘要： A compound of formula (I) wherein R1 is hydrogen, methyl, ethyl, methoxy or methylthio; R2 and R3 each independently is hydrogen or C1-3 alkyl; R4 is hydrogen, lower alkyl, methoxy, ethoxy, or benzyloxy; R5 is lower alkyl, lower cycloalkyl, (CH2)mC(O)OR6 wherein m is the integer 1 or 2 and R6 is lower alkyl, phenyl optionally substituted with C(O)OR7 wherein R7 is lower alkyl or phenyl(lower alkyl); or R6 is Het or Het(lower alkyl); or R4 and R5 together with the nitrogen atom to which they are attached form a nitrogen containing ring optionally substituted with benzyloxycarbonyl or with phenyl optionally substituted among other group with C(O)OR7 wherein R7 is lower alkyl or (lower alkyl)phenyl; X is selected from the group consisting of O, S, SO, SO2, NR8, wherein R8 is H or lower alkyl; and Y is C1-10 non-cyclic or cyclic alkyl; [(CH2)0-1]-phenyl, said phenyl ring optionally substituted; Het or Het(lower alkyl); or when X is NR8, wherein R8 is lower alkyl and Y is lower alkyl or lower alkoxy, X and Y are joined together to form a morpholino or piperidino ring; or a therapeutically acceptable acid addition salt thereof.

46. 发明公开

EP1260222A1 Butenyl-substituted taxanes and composition 失效
标题翻译：含新颖异丁烯基取代的紫杉烷的药物组合物
公开(公告)号：EP1260222A1
公开(公告)日：2002-11-27
申请号：EP02019283.7
申请日：1993-11-01
申请人： Florida State University
发明人： The designation of the inventor has not yet been filed
IPC分类号： A61K31/335 , C07D305/14 , C07D205/08 , A61P35/00
CPC分类号： C07D305/14
摘要： Pharmaceutical compositions are described which contain butenyl-substituted taxanes.
摘要翻译：药物组合物描述了含有丁烯substituiertem紫杉烷类。

47. 发明公开

EP1256572A1 Process for the deprotection of N-substituted azetidones 审中-公开
标题翻译： Verfahren zumentschützenvon N-substitutionierten Azetidonen
公开(公告)号：EP1256572A1
公开(公告)日：2002-11-13
申请号：EP01870100.3
申请日：2001-05-10
申请人： Tessenderlo Chemie S.A.
发明人： Ceresiat, Marcel Maurice Ghislain , Belmans, Marc , Marchand-Brynaert, Jaqueline , Laurent, Mathieu
IPC分类号： C07D205/08
CPC分类号： C07D205/08 , Y02P20/55
摘要： The present invention relates to a method for the preparation of a compound of the general formula (I) wherein

R 1 and R 2 each represent independently hydrogen, halogen, hydroxy, thiol, nitro, amino, carboxy, amino derivative, oxy derivative, thio derivative, alkyl, alkenyl, alkynyl, aryl, oxy derivative, amino derivative, thiol derivative, acyl derivative, acyloxy derivative, ester, amido, ether, arylalkyl, heterocycle or Me(OR')CH wherein R' is hydrogen or R a R b R c Si wherein R a , R b and R c is independently chosen from the group consisting of alkyl, alkenyl, alkynyl, aryl or a heterocycle;
R 3 represents a protecting group such as alkyl, alkenyl, alkynyl, or arylalkyl;
wherein this method comprises the reaction of a compound of the general formula (II) in the presence of a halogen-radical source, water and a proton donor suitable as a catalyst.
摘要翻译：本发明涉及制备通式（I）的化合物的方法，其中R 1和R 2各自独立地代表氢，卤素，羟基，硫醇，硝基，氨基，羧基，氨基衍生物，氧基衍生物，硫代衍生物，烷基，烯基，炔基，芳基，氧基衍生物，氨基衍生物，硫醇衍生物，酰基衍生物，酰氧基衍生物，酯，酰胺基，醚，芳基烷基，杂环或Me（OR'）CH，其中R' 或R a R c R c Si，其中R a，R b和R c独立地选自烷基，烯基，炔基，芳基或杂环; R 3表示保护基如烷基，烯基，炔基或芳基烷基; 其中该方法包括通式（II）的化合物在卤素自由基源，水和适合作为催化剂的质子给体存在下的反应。

48. 发明授权

EP0755937B1 Phosphine-phosphinite compound and process for preparing 4-[(R)-1'-formylethyl]-azetidin-2-one derivatives using the same 失效
标题翻译：膦次亚膦酸酯化合物和为4的制备方法 - 氮杂环丁-2-酮使用这些化合物的衍生物（（R）-1'-甲酰基乙基）
公开(公告)号：EP0755937B1
公开(公告)日：2002-10-23
申请号：EP96305182.6
申请日：1996-07-15
申请人： Takasago International Corporation
发明人： Saito, Takao , Matsumura, Kazuhiko , Miura, Takashi , Kumobayashi, Hidenori , Yoshida, Akifumi, c/o Takasago Int. Corp.
IPC分类号： C07F9/46 , C07D205/08
CPC分类号： C07F9/65517 , C07D205/08 , C07F9/5022 , Y02P20/55

49. 发明授权

EP0792264B1 SULFUR-SUBSTITUTED AZETIDINONE COMPOUNDS USEFUL AS HYPOCHOLESTEROLEMIC AGENTS 失效
标题翻译：硫取代的AZETDINONE HYPOCHOLESTEROLMISCHMITTEL
公开(公告)号：EP0792264B1
公开(公告)日：2002-02-27
申请号：EP95939677.1
申请日：1995-11-15
申请人： SCHERING CORPORATION
发明人： McKITTRICK, Brian, A. , DUGAR, Sundeep , BURNETT, Duane, A.
IPC分类号： C07D205/08 , C07D409/12 , C07D401/12 , A61K31/395 , A61K31/44
CPC分类号： C07D401/12 , C07D205/08 , C07D409/12
摘要： Sulfur-substituted azetidinone hypocholesterolemic agents of formula (I), or a pharmaceutically acceptable salt thereof, wherein: Ar1 is aryl, R10-substituted aryl or heteroaryl; Ar2 is aryl or R4-substituted aryl; Ar3 is aryl or R5-substituted aryl; X and Y are -CH¿2?-, -CH(lower alkyl)- or -C(dilower alkyl)-; R is -OR?6¿, -O(CO)R6, -O(CO)OR9 or -O(CO)NR6R7; R1 is hydrogen, lower alkyl or aryl; or R and R1 together are =0; q is 0 or 1; r is 0, 1 or 2; m and n are 0-5; provided that the sum of m, n and q is 1-5; R4 is selected from lower alkyl, -OR6, -O(CO)R6, -O(CO)OR9, -O(CH¿2?)1-5OR?6¿, -O(CO)NR?6R7, -NR6R7, -NR6(CO)R7, -NR6(CO)OR9, -NR6(CO)NR7R8, -NR6SO¿2R?9, -COOR6, -CONR6R7, -COR6, -SO¿2NR6R7, S(O)¿0-2R?9, -O(CH¿2?)1-10-COOR?6¿, -O(CH¿2?)1-10CONR?6R7¿, -(lower alkylene)-COOR6 and -CH=CH-COOR6; R5 is selected from -OR6, -O(CO)R6, -O(CO)OR9, -O(CH¿2?)1-5OR?6¿, -O(CO)NR?6R7, -NR6?R?7 -NR6(CO)R7, -NR6(CO)OR9, -NR6(CO)NR7R8, -NR6SO¿2R?9, -COOR6, -CONR6R7, -COR6, -SO¿2NR6R7, S(O)¿0-2R?9, -O(CH¿2?)1-10-COOR?6¿, -O(CH¿2?)1-10CONR?6R7, -CF¿3, -CN, -NO2, halogen, -(lower alkylene)COOR6 and -CH=CH-COOR?6; R6, R7 and R8¿ are H, lower alkyl, aryl or aryl-substitued lower alkyl; R9 is lower alkyl, aryl or aryl-sybstituted lower alkyl; and R10 is selected from lower alkyl, -OR6, -O(CO)R6, -O(CO)OR9, -O(CH¿2?)1-5OR?6¿, -O(CO)NR?6R7, -NR6R7, -NR6(CO)R7, -NR6(CO)OR9, -NR6(CO)NR7R8, -NR6SO¿2R?9, -COOR6, -CONR6R7, COR6, -SO¿2NR6R7, -S(O)¿0-2R?9, -O(CH¿2?)1-10-COOR?6¿, -O(CH¿2?)1-10CONR?6R7, -CF¿3, -CN, -NO2 and halogen; are disclosed, as well as pharmaceutical compositions containing them, and a method of lowering serum cholesterol by administering said compounds, alone or in combination with a cholesterol biosynthesis inhibitor.

50. 发明授权

EP0707567B1 PROCESS FOR THE SYNTHESIS OF AZETIDINONES 失效
标题翻译：合成吖啶酮的方法
公开(公告)号：EP0707567B1
公开(公告)日：2001-09-12
申请号：EP94921407.6
申请日：1994-07-01
申请人： SCHERING CORPORATION
发明人： THIRUVENGADAM, Tiruvettipuram, Kannapan , McALLISTER, Timothy , TANN, Chou-Hong
IPC分类号： C07D205/08
CPC分类号： C07D205/08

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