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1. 发明授权

US06395895B1 Butenyl substituted &bgr;-lactams 失效
标题翻译：丁烯基取代的β-内酰胺
公开(公告)号：US06395895B1
公开(公告)日：2002-05-28
申请号：US09427973
申请日：1999-10-27
申请人： Robert A. Holton , Ki-byung Chai , Hossain Nadizadeh
发明人： Robert A. Holton , Ki-byung Chai , Hossain Nadizadeh
IPC分类号： C07D20508
CPC分类号： C07D407/12 , C07C227/22 , C07C231/12 , C07C233/87 , C07C2601/14 , C07C2601/16 , C07C2603/62 , C07D205/08 , C07D305/14 , C07D409/12 , C07F7/003 , C07F7/1804
摘要： Taxane derivatives having a 3′ butenyl substituted C13 side chain.
摘要翻译：具有3'丁烯基取代的C13侧链的紫杉烷衍生物

2. 发明授权

US06239125B1 Azetidinone derivatives for the treatment of HCMV infections 有权
标题翻译：氮杂环丁酮衍生物用于治疗HCMV感染
公开(公告)号：US06239125B1
公开(公告)日：2001-05-29
申请号：US09167142
申请日：1998-10-06
申请人： Eric Malenfant , Jeffrey O'Meara , Robert Déziel , William W. Ogilvie
发明人： Eric Malenfant , Jeffrey O'Meara , Robert Déziel , William W. Ogilvie
IPC分类号： C07D20508
CPC分类号： C07D401/12 , A61K31/395 , A61K31/70 , A61K45/06 , C07D205/08 , C07D205/09
摘要： A compound of formula 1: wherein Y is S or O; R1 is C1-6 alkyl; (C0-6 alkyl)aryl; (C0-6 alkyl)Het; or R1 is an amino acid analog or dipeptide analog of the formula: wherein R2 is H, C1-10 alkyl; or an amide or ester group; A is C6-10 aryl, Het or CH—R3 wherein R3 is C1-6 alkyl or (C0-4 alkyl)aryl; and Z is H, C1-6 alkyl, or an acyl; R4 is hydrogen, lower alkyl, methoxy, ethoxy, or benzyloxy; and R5 is alkyl, cycloalkyl, carboxyl group; an aryl; 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 phenyl or C(O)OCH2-phenyl, said phenyl ring optionally mono- or di-substituted with among others C(O)OR7 wherein R7 is lower alkyl or phenyl(lower alkyl); or a therapeutically acceptable acid addition salt thereof which compounds are useful in the treatment of HCMV infections.
摘要翻译：式1的化合物：其中Y是S或O; R 1是C 1-6烷基; （C0-6烷基）芳基; （C0-6烷基）Het; 或R 1是下式的氨基酸类似物或二肽类似物：其中R 2是H，C 1-10烷基; 或酰胺或酯基; A为C 6-10芳基，Het或CH-R 3，其中R 3为C 1-6烷基或（C 0-4烷基）芳基; 和Z是H，C 1-6烷基或酰基; R 4是氢，低级烷基，甲氧基，乙氧基或苄氧基; 和R 5是烷基，环烷基，羧基; 芳基; Het或Het（低级烷基）; 或R 4和R 5与它们所连接的氮原子一起形成任选被苯基或C（O）OCH 2 - 苯基取代的含氮环，所述苯环任选地被C（O）OR 7单取代，其中 R7是低级烷基或苯基（低级烷基）; 或其治疗上可接受的酸加成盐，其化合物可用于治疗HCMV感染。

3. 发明授权

US06211170B1 Azetidinone derivatives for the treatment of HCMV infections 有权
标题翻译：氮杂环丁酮衍生物用于治疗HCMV感染
公开(公告)号：US06211170B1
公开(公告)日：2001-04-03
申请号：US09167141
申请日：1998-10-06
申请人： Christiane Yoakim , Robert Déziel , Stephen Kawai , William W. Ogilvie , Jeffrey O'Meara , Catherine Chabot
发明人： Christiane Yoakim , Robert Déziel , Stephen Kawai , William W. Ogilvie , Jeffrey O'Meara , Catherine Chabot
IPC分类号： C07D20508
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, which compound is useful in the treatment of HCMV infection.
摘要翻译：式I的化合物：其中R 1是氢，甲基，乙基，甲氧基或甲硫基; R2和R3各自独立地为氢或C1-3烷基; R4是氢，低级烷基，甲氧基，乙氧基或苄氧基; R5是低级烷基，低级环烷基，（CH2）mC（O）OR6，其中m是整数1或2，R6是低级烷基，任选被C（O）OR 7取代的苯基，其中R 7是低级烷基或苯基（低级烷基） ; 或R6是Het或Het（低级烷基;或R4和R5与它们所连接的氮原子一起形成任选被苄氧基羰基取代的含氮环或与C（O）OR 7任选取代的苯基，其中R 7是低级烷基或（低级烷基）苯基; X选自O，S，SO，SO 2，NR 8，其中R 8为H或低级烷基; Y为C 1-10非环状或环状烷基; [（CH 2 ）0-1] - 苯基，所述苯环任选被取代; Het或Het（低级烷基）;或当X是NR8时，其中R8是低级烷基，Y是低级烷基或低级烷氧基，X和Y连接在一起形成吗啉或哌啶子基环;或其治疗上可接受的酸加成盐，该化合物可用于治疗HCMV感染。

4. 发明授权

US06730782B2 Carbamoyl substituted &bgr;-lactams 失效
标题翻译：氨基甲酰取代的β-内酰胺
公开(公告)号：US06730782B2
公开(公告)日：2004-05-04
申请号：US10082755
申请日：2002-02-25
申请人： Robert A. Holton , Hossain Nadizadeh , Kasthuri Rengan , Chunlin Tao
发明人： Robert A. Holton , Hossain Nadizadeh , Kasthuri Rengan , Chunlin Tao
IPC分类号： C07D20508
CPC分类号： C07D407/12 , C07C227/22 , C07C231/12 , C07C233/87 , C07C2601/14 , C07C2601/16 , C07C2603/62 , C07D205/08 , C07D305/14 , C07D409/12 , C07F7/003 , C07F7/1804
摘要： Taxane derivatives having an amino substituted C13 side chain.
摘要翻译：具有氨基取代的C13侧链的紫杉烷衍生物。

5. 发明授权

US06242596B1 Preparation of betamethyl carbapenem intermediates 失效
标题翻译：二甲基碳青霉烯中间体的制备
公开(公告)号：US06242596B1
公开(公告)日：2001-06-05
申请号：US08241958
申请日：1994-05-12
申请人： Woo-Baeg Choi , Guy R. Humphrey , Paul J. Reider , Ichiro Shinkai , Andrew S. Thompson , Ralph P. Volante
发明人： Woo-Baeg Choi , Guy R. Humphrey , Paul J. Reider , Ichiro Shinkai , Andrew S. Thompson , Ralph P. Volante
IPC分类号： C07D20508
CPC分类号： C07D405/04 , C07D205/08 , Y02P20/55
摘要： A process for making a beta methyl carbapenem intermediate is disclosed. A compound of formula I: is contacted in a non-reactive solvent with methyl Meldrum's acid and a base to produce a compound of formula III: Compound III is treated in an aprotic solvent with a scavenging base, an alkali metal halide and a tri-organo silyl protecting compound for nitrogen to produce a compound of formula IV: Compound IV may be reacted with a nucleophile Nu—X in a non-reactive solvent and base, and the mixture acidified to produce a compound of formula V. Compound V may be reacted with mild acid to produce a compound of formula VI.
摘要翻译：公开了一种制备β-甲基碳青霉烯中间体的方法。将式I化合物在非反应性溶剂中与甲基Meldrum酸和碱接触以产生式III化合物：化合物III在非质子溶剂中用清除碱，碱金属卤化物和三 - 用于氮的有机甲硅烷基保护化合物以产生式IV的化合物：化合物IV可以在非反应性溶剂和碱中与亲核试剂Nu-X反应，并将该混合物酸化以产生式V化合物。化合物V可以是与轻度酸反应生成式Ⅵ化合物。

6. 发明授权

US06610680B1 Non-peptidyl vasopressin V1A antagonists 有权
标题翻译：非肽基血管加压素V1A拮抗剂
公开(公告)号：US06610680B1
公开(公告)日：2003-08-26
申请号：US10327240
申请日：2002-12-20
申请人： Robert F Bruns, Jr. , Robin D G Cooper , Bruce A Dressman , David C Hunden , Stephen W Kaldor , Gary A Koppel , John R Rizzo , Jeffrey J Skelton , Mitchell I Steinberg
发明人： Robert F Bruns, Jr. , Robin D G Cooper , Bruce A Dressman , David C Hunden , Stephen W Kaldor , Gary A Koppel , John R Rizzo , Jeffrey J Skelton , Mitchell I Steinberg
IPC分类号： C07D20508
CPC分类号： C07D413/04 , C07D413/14
摘要： This invention provides substituted 2-(azetidinon-1-yl) acetic acid derivatives of Formula II for the antagonism of the vasopressin V1a receptor.
摘要翻译：本发明提供式II的取代的2-（氮杂环丁烷-1-基）乙酸衍生物用于加压素V1a受体的拮抗作用。

7. 发明授权

US06407228B1 Method for the preparation of &bgr;-lactam compound 失效
标题翻译： β-内酰胺化合物的制备方法
公开(公告)号：US06407228B1
公开(公告)日：2002-06-18
申请号：US08527217
申请日：1995-09-12
申请人： Yoichi Taguchi , Akihiro Oishi , Isao Shibuya , Tohru Tsuchiya
发明人： Yoichi Taguchi , Akihiro Oishi , Isao Shibuya , Tohru Tsuchiya
IPC分类号： C07D20508
CPC分类号： C07D201/02 , C07D205/08
摘要： A simple and efficient method is proposed for the preparation of a &bgr;-lactam compound such as 1-phenyl-4-ethoxy-2-azetidinone which can be produced by mixing an isocyanate compound such as phenyl isocyanate and a vinyl ether compound such as ethyl vinyl ether and heating the mixture at a moderate temperature under a superatmospheric pressure of up to 12000 atmospheres.
摘要翻译：提出了一种制备β-内酰胺化合物如1-苯基-4-乙氧基-2-氮杂环丁酮的简单且有效的方法，其可以通过将异氰酸酯化合物如异氰酸苯酯和乙烯基醚化合物如乙基乙烯基醚，并在中等温度下在高达12000个大气压的超大气压下加热该混合物。

8. 发明授权

US06333418B1 Cyclisation process 失效
标题翻译：循环过程
公开(公告)号：US06333418B1
公开(公告)日：2001-12-25
申请号：US09380293
申请日：1999-08-31
申请人： Julian Simon Parratt , Stephen John Clifford Taylor
发明人： Julian Simon Parratt , Stephen John Clifford Taylor
IPC分类号： C07D20508
CPC分类号： C07D205/08
摘要： There is provided a process for the cyclisation of 4-amino-2-halobutyric acid to azetidine-2-carboxylic acid wherein more than 20 g of 4-amino-2-halobutyric acid is cyclised per liter of reaction mixture.
摘要翻译：提供了将4-氨基-2-卤代丁酸环化为氮杂环丁烷-2-羧酸的方法，其中每升反应混合物环化多于20g的4-氨基-2-卤代丁酸。

9. 发明授权

US06187916B1 Process for the preparation of taxane derivatives and &bgr;-lactam intermediates therefor 失效
标题翻译：紫杉烷衍生物和β-内酰胺中间体的制备方法
公开(公告)号：US06187916B1
公开(公告)日：2001-02-13
申请号：US08481205
申请日：1995-06-07
申请人： Iwao Ojima
发明人： Iwao Ojima
IPC分类号： C07D20508
CPC分类号： C07D305/14 , C07D205/08
摘要： A process for the preparation of a taxane derivative of the formula in which R2 represents an RO—, RS— or RR′N— in which R represents an unsubstituted or substituted straight chain or branched alkyl, alkenyl or alkynyl, or cycloalkyl, saturated heterocyclic, cycloalkenyl, unsaturated heterocyclic, aryl or heterocyclic aromatic; R′ is a hydrogen or R defined above; R and R′ can be connected to form together with the nitrogen a cyclic structure; Y is oxygen or sulfur; R3 represents an unsubstituted or substituted straight chain or branched alkyl, alkenyl or alkynyl radical, an unsubstituted or substituted cycloalkyl, cycloalkenyl or an unsubstituted or substituted aryl; which comprises reacting a &bgr;-lactam of the formula in which R311 represents a radical R3 defined above or a protected R3 whenever R3 includes one or more active hydrogens; with a baccatin III derivative of the formula: in which M is an alkali metal or alkaline earth metal atom (ion).
摘要翻译：一种制备甲醛的紫杉烷衍生物的方法，其中R 2表示RO-，RS-或RR'N-，其中R表示未取代或取代的直链或支链烷基，烯基或炔基或环烷基，饱和杂环，环烯基，不饱和杂环，芳基或杂环芳族; R'是上面定义的氢或R; R和R'可以与氮一起形成环状结构; Y是氧或硫; R3表示未取代或取代的直链或支链烷基，烯基或炔基，未取代或取代的环烷基，环烯基或未取代的或取代的芳基;其包括使R 3 11表示上述定义的基团R 3的β-内酰胺或每当R 3包括一个或多个活性氢时被保护的R3反应; 与下式的浆果赤霉素III衍生物：其中M是碱金属或碱土金属原子（离子）。

10. 再颁专利

USRE37721E1 Hydroxy-substituted azetidinone compounds useful as hypocholesterolemic agents 有权
标题翻译：用作降胆固醇药的羟基取代的氮杂环丁酮化合物
公开(公告)号：USRE37721E1
公开(公告)日：2002-05-28
申请号：US09594996
申请日：2000-06-15
申请人： Stuart B. Rosenblum , Sundeep Dugar , Duane A. Burnett , John W. Clader , Brian A. McKittrick
发明人： Stuart B. Rosenblum , Sundeep Dugar , Duane A. Burnett , John W. Clader , Brian A. McKittrick
IPC分类号： C07D20508
CPC分类号： C07D205/08 , A61K9/2018 , A61K9/4858 , A61K31/21 , A61K31/35 , A61K31/395 , A61K31/40 , A61K45/06 , Y02P20/55 , Y10S514/824 , A61K2300/00
摘要： Hydroxy-substituted azetidinone hypocholesterolemic agents of the formula or a pharmaceutically acceptable salt thereof, wherein: Ar1 and Ar2 are aryl or R4-substituted aryl; Ar3 is aryl or R5-substituted aryl; X, Y and Z are —CH2—, —CH(lower alkyl)— or —C(dilower alkyl)—; R and R2 are —OR6, —O(CO)R6, —O(CO)OR9 or —O(CO)NR6R7; R1 and R3 are H or lower alkyl; q is 0 or 1; r is 0 or 1; m, n and p are 0-4; provided that at least one of q and r is 1, and the sum of m, n, p, q and r is 1-6; and provided that when p is O and r is 1, the sum of m, q and n is 1-5; R4 is selected from lower alkyl, R5, —CF3, —CN, —NO2 and halogen R5 is selected from —OR6, —O(CO)R6, —O(CO)OR9, —O(CH2)1-5OR6, —O(CO)NR6R7, —NR6R7, —NR6(CO)R7, —NR6(CO)OR9, —NR6(CO)NR7R8, —NR6SO2R9, —COOR6, —CONR6R7, —COR6, —SO2NR6R7, S(O)0-2R9, —O(CH2)1-10—COOR6, —O(CH2)1-10CONR6R7, —(lower alkylene)COOR6 and —CH═CH—COOR6; R6, R7 and R8 are H, lower alkyl or aryl-substituted Ic R9 is lower alkyl, aryl or aryl-substituted lower alkyl; are disclosed, as well as a method of lowering serum cholesterol by administering said compounds, alone or in combination with a cholesterol biosynthesis inhibitor, pharmaceutical compositions containing them; and a process for preparing them.
摘要翻译：羟基取代的氮杂环丁酮低胆固醇血症药或其药学上可接受的盐，其中：Ar1和Ar2是芳基或R4取代的芳基; Ar3是芳基或R5-取代的芳基; X，Y和Z是-CH2-，-CH（低级烷基） - 或-C（二卤代烷基） - ; R和R 2为-OR 6，-O（CO）R 6，-O（CO）OR 9或-O（CO）NR 6 R 7; R 1和R 3为H或低级烷基; q为0或1; r为0或1; m，n和p为0-4; 条件是q和r中的至少一个为1，m，n，p，q和r的和为1-6; 并且条件是当p为O且r为1时，m，q和n的和为1-5; R 4选自低级烷基，R 5，-CF 3，-CN，-NO 2，卤素R 5选自-OR 6 ，-O（CO）R 6，-O（CO）OR 9，-O（CH 2）1-5 OR 6，-O（CO）NR 6 R 7，-NR 6 R 7，-NR 6（CO）R 7，-NR 6（CO）OR 9，-NR 6 （CO）NR7R8，-NR6SO2R9，-COOR6，-CONR6R7，-COR6，-SO2NR6R7，S（O）0-2R9，-O（CH2）1-10-COOR6，-O（CH2）1-10CONR6R7， - （低级亚烷基）COOR 6和-CH = CH-COOR 6; R6，R7和R8是H，低级烷基或芳基取代的IcR9是低级烷基，芳基或芳基取代的低级烷基;以及降低血清的方法通过单独或与胆固醇生物合成抑制剂组合施用所述化合物，含有它们的药物组合物; 和一个准备它们的过程。

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