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1. 发明授权

US6025177A Asymmetric grignard synthesis with cyclic 1,2 aminoalcohols 失效
标题翻译：不对称格氏合成与环状1,2氨基醇
公开(公告)号：US6025177A
公开(公告)日：2000-02-15
申请号：US247731
申请日：1999-02-09
申请人： Chris Hugh Senanayake , Roger P. Bakale , Qun Kevin Fang , Paul Timothy Grover , Donald L. Heefner , Richard F. Rossi , Stephen Alan Wald
发明人： Chris Hugh Senanayake , Roger P. Bakale , Qun Kevin Fang , Paul Timothy Grover , Donald L. Heefner , Richard F. Rossi , Stephen Alan Wald
IPC分类号： C07C215/44 , C07C311/20 , C07D263/52 , C07D263/08
CPC分类号： C07D263/52 , C07C215/44 , C07C311/20 , C07C2101/14 , C07C2102/08 , Y02P20/582
摘要： Processes for preparing a single enantiomer of an .alpha.,.alpha.-disubstituted-.alpha.-hydroxy acetic acid, especially cyclohexylphenylglycolic acid (CHPGA), is disclosed. The processes employ cyclic 1,2-aminoalcohols as chiral auxiliaries by forming diastereomeric esters of aminoalcohols or diastereomeric amides of oxazolidines. ##STR1## Intermediates useful in the process are also disclosed.
摘要翻译：公开了制备α，α-二取代-α-羟基乙酸，特别是环己基苯基乙醇酸（CHPGA）的单一对映异构体的方法。该方法通过形成恶唑烷的氨基醇或非对映体酰胺的非对映异构体酯，将环状1,2-氨基醇用作手性助剂。还公开了在该方法中有用的中间体。

2. 发明授权

US6013830A Asymmetric grignard synthesis with cyclic 1,2 aminoalcohols 失效
公开(公告)号：US6013830A
公开(公告)日：2000-01-11
申请号：US050825
申请日：1998-03-30
申请人： Chris Hugh Senanayake , Roger P. Bakale , Qun Kevin Fang , Paul Timothy Grover , Donald L. Heefner , Richard F. Rossi , Stephen Alan Wald
发明人： Chris Hugh Senanayake , Roger P. Bakale , Qun Kevin Fang , Paul Timothy Grover , Donald L. Heefner , Richard F. Rossi , Stephen Alan Wald
IPC分类号： C07C215/44 , C07C311/20 , C07D263/52 , C07C69/76 , C07D263/54
CPC分类号： C07D263/52 , C07C215/44 , C07C311/20 , C07C2101/14 , C07C2102/08 , Y02P20/582
摘要： Processes for preparing a single enantiomer of an .alpha.,.alpha.-disubstituted-.alpha.-hydroxy acetic acid, especially cyclohexylphenylglycolic acid (CHPGA), is disclosed. The processes employ cyclic 1,2-aminoalcohols as chiral auxiliaries by forming diastereomeric esters of aminoalcohols or diastereomeric amides of oxazolidines. ##STR1## Intermediates useful in the process are also disclosed.

3. 发明授权

US06207679B1 Antimicrobial agents uses and compositions related thereto 失效
标题翻译：抗微生物剂用途及其组合物
公开(公告)号：US06207679B1
公开(公告)日：2001-03-27
申请号：US09045051
申请日：1998-03-19
申请人： Gregory D. Cuny , James R. Hauske , Donald L. Heefner , Michael Z. Hoemann , Gnanasambandam Kumaravel , Anita Melikian-Badalian , Richard F. Rossi
发明人： Gregory D. Cuny , James R. Hauske , Donald L. Heefner , Michael Z. Hoemann , Gnanasambandam Kumaravel , Anita Melikian-Badalian , Richard F. Rossi
IPC分类号： A61K314709
CPC分类号： C07D401/14 , C07D209/12 , C07D209/14 , C07D215/52 , C07D401/04 , C07D405/04 , C07D409/04 , C07D471/04 , C07D491/04
摘要： The present invention provides methods and pharmaceutical preparations that inhibit the growth of bacterial microorganisms. Additionally, the present invention provides methods and pharmaceutical preparations that kill bacterial microorganisms.
摘要翻译：本发明提供抑制细菌微生物生长的方法和药物制剂。此外，本发明提供杀死细菌微生物的方法和药物制剂。

4. 发明授权

US5529929A Optical resolution of alkyl 1,4-benzodioxan-2-carboxylates using esterase from serratia marcescens 失效
标题翻译：使用来自粘质沙雷氏菌的酯酶对1,4-苯并二恶烷-2-羧酸烷基酯进行光学拆分
公开(公告)号：US5529929A
公开(公告)日：1996-06-25
申请号：US477381
申请日：1995-06-07
申请人： Richard F. Rossi, Jr. , Charles M. Zepp , Donald L. Heefner
发明人： Richard F. Rossi, Jr. , Charles M. Zepp , Donald L. Heefner
IPC分类号： C12P17/06 , C12P41/00
CPC分类号： C12P17/06 , C12P41/005 , Y10S435/881
摘要： A process for resolving racemic alkyl 1,4-benzodioxan-2-carboxylates useful as intermediates in the synthesis of optically pure pharmaceutical compounds such as (S)-doxazosin is disclosed. The process utilizes a microbial enzyme derived from Serratia marcescens to catalyze the enantioselective hydrolysis of the alkyl (S)-1,4-benzodioxan-2-carboxylate enantiomer of the racemic mixture to its corresponding carboxylic acid at a faster rate than the R-enantiomer. An enantiomerically pure S-configured carboxylic acid is thereby formed for subsequent pharmaceutical synthesis. The nonhydrolyzed alkyl (R)-1,4-benzodioxan-2-carboxylate enantiomer can also be isolated and racemized, and the enzymatic hydrolysis reaction repeated.
摘要翻译：公开了用于合成光学纯药物化合物如（S） - 恶唑嗪的中间体的外消旋烷基1,4-苯并二恶烷-2-羧酸酯的方法。该方法利用来自粘质沙雷氏菌的微生物酶催化外消旋混合物的（S）-1,4-苯并二恶烷-2-羧酸烷基酯对映异构体对映选择性水解速率比R对映异构体。由此形成对映异构体纯的S-构型的羧酸用于随后的药物合成。还可以分离非水解的（R）-1,4-苯并二恶烷-2-羧酸烷基酯对映异构体并进行外消旋化，并重复酶水解反应。

5. 发明授权

US5273895A Enantioselective production of chiral carboxylic acids 失效
标题翻译：对映选择性生产手性羧酸
公开(公告)号：US5273895A
公开(公告)日：1993-12-28
申请号：US966705
申请日：1992-10-26
申请人： Richard F. Rossi , Donald L. Heefner , Charles M. Zepp
发明人： Richard F. Rossi , Donald L. Heefner , Charles M. Zepp
IPC分类号： C12P7/40 , C12P41/00 , C12R1/01 , C12R1/02 , C12R1/025 , C12R1/05 , C12R1/06 , C12R1/07 , C12R1/13 , C12R1/185 , C12R1/38 , C12R1/425 , C12R1/66 , C12R1/72 , C12R1/85 , C12N9/02
CPC分类号： C12P41/002 , C12P7/40
摘要： A process for enantioselectively converting an aldehyde, a bisulfite adduct of an aldehyde or a glycidate to a chiral carboxylic acid is disclosed. The process utilizes a microorganism or an enzyme preparation from a microorganism and is particularly useful for producing NSAIDs of the profen class from readily available precursors. Preferred microorganisms are Gram-negative rod bacteria.
摘要翻译：公开了将醛，醛或缩水甘油酸的亚硫酸氢盐加合物对映选择性转化成手性羧酸的方法。该方法利用来自微生物的微生物或酶制剂，并且特别可用于从容易获得的前体产生等级的NSAID。优选的微生物是革兰氏阴性杆菌。

6. 发明授权

US06172084B2 Quinoline-indole antimicrobial agents, uses and compositions related thereto 失效
标题翻译：喹啉 - 吲哚抗微生物剂，其用途和组合物
公开(公告)号：US06172084B2
公开(公告)日：2001-01-09
申请号：US09099640
申请日：1998-06-18
申请人： Gregory D. Cuny , James R. Hauske , Donald L. Heefner , Michael Z. Hoemann , Gnanasambandam Kumaravel , Anita Melikian-Badalian , Richard F. Rossi
发明人： Gregory D. Cuny , James R. Hauske , Donald L. Heefner , Michael Z. Hoemann , Gnanasambandam Kumaravel , Anita Melikian-Badalian , Richard F. Rossi
IPC分类号： A61K3147
CPC分类号： C07D401/14 , C07D209/12 , C07D209/14 , C07D215/52 , C07D401/04 , C07D405/04 , C07D409/04 , C07D471/04 , C07D491/04
摘要： The present invention provides methods and pharmaceutical preparations that inhibit the growth of bacterial microorganisms. Additionally, the present invention provides methods and pharmaceutical preparations that kill bacterial microorganisms.
摘要翻译：本发明提供抑制细菌微生物生长的方法和药物制剂。此外，本发明提供杀死细菌微生物的方法和药物制剂。

7. 发明授权

US6103905A Quinoline-indole antimicrobial agents, uses and compositions related thereto 失效
标题翻译：喹啉 - 吲哚抗微生物剂，其用途和组合物
公开(公告)号：US6103905A
公开(公告)日：2000-08-15
申请号：US213385
申请日：1998-12-11
申请人： Gregory D. Cuny , James R. Hauske , Donald L. Heefner , Michael Z. Hoemann , Gnanasambandam Kumaravel , Anita Melikian-Badalian , Richard F. Rossi , Roger L. Xie
发明人： Gregory D. Cuny , James R. Hauske , Donald L. Heefner , Michael Z. Hoemann , Gnanasambandam Kumaravel , Anita Melikian-Badalian , Richard F. Rossi , Roger L. Xie
IPC分类号： C07D209/12 , C07D209/14 , C07D215/52 , C07D401/04 , C07D401/14 , C07D405/04 , C07D405/14 , C07D409/04 , C07D453/02 , C07D471/04 , C07D491/04 , A61K31/47 , C07D265/30 , C07D295/06
CPC分类号： C07D401/14 , C07D209/12 , C07D209/14 , C07D215/52 , C07D401/04 , C07D405/04 , C07D405/14 , C07D409/04 , C07D453/02 , C07D471/04 , C07D491/04
摘要： The present invention provides methods and pharmaceutical preparations that inhibit the growth of bacteria microorganisms. Additionally, the present invention provides methods and pharmaceutical preparations that kill bacterial microorganisms.
摘要翻译：本发明提供抑制细菌微生物生长的方法和药物制剂。此外，本发明提供杀死细菌微生物的方法和药物制剂。

8. 发明授权

US5658796A Optical resolution of alkyl chroman-2-carboxylates 失效
标题翻译：烷基色满-2-羧酸酯的光学拆分
公开(公告)号：US5658796A
公开(公告)日：1997-08-19
申请号：US475007
申请日：1995-06-07
申请人： Richard F. Rossi, Jr. , Charles M. Zepp , Donald L. Heefner
发明人： Richard F. Rossi, Jr. , Charles M. Zepp , Donald L. Heefner
IPC分类号： C07D311/66 , C12P41/00
CPC分类号： C07D311/66 , C12P41/004 , Y10S435/881
摘要： Described herein is a process for resolving a racemic (C>3) alkyl (R, S) chroman-2-carboxylate compound useful as intermediates in the synthesis of optically pure pharmaceutical compounds is disclosed. The process utilizes a microbial enzyme derived from Serratia marcescens to catalyze the enantioselective hydrolysis of the (C>3) alkyl (S)-chroman-2-carboxylate enantiomer of the racemic mixture to its corresponding carboxylic acid at a faster rate than the R-enantiomer. An enantiomerically pure S-configured carboxylic acid is thereby formed which can undergo acidic esterification to provide an optically pure (C>3) alkyl (S)-chroman-2-carboxylate intermediate for subsequent pharmaceutical synthesis. The nonhydrolyzed (C>3) alkyl (R)-chroman-2-carboxylate enantiomer can also be isolated to provide an optically pure pharmaceutical precursor.
摘要翻译：本文描述了一种拆分用作光学纯药物化合物合成中的中间体的外消旋（C 3）烷基（R 3，S）色满-2-羧酸酯化合物的方法。该方法利用来自粘质沙雷氏菌的微生物酶催化外消旋混合物的（C 3）烷基（S） - 苯并二氢吡喃-2-羧酸酯对映异构体对映体选择性水解速率比R- 对映体。由此形成对映异构体纯的S-构型的羧酸，其可进行酸性酯化以提供用于随后的药物合成的光学纯的（C 3）烷基（S） - 苯并二氢吡喃-2-羧酸酯中间体。也可以分离非水解（C 3）烷基（R） - 苯并二氢吡喃-2-羧酸酯对映异构体以提供光学纯的药物前体。

9. 发明授权

US6063562A In vitro method for predicting the evolutionary response of HIV protease to a drug targeted thereagainst 失效
公开(公告)号：US6063562A
公开(公告)日：2000-05-16
申请号：US420003
申请日：1995-04-10
申请人： Laurence M. Melnick , Donald L. Heefner
发明人： Laurence M. Melnick , Donald L. Heefner
IPC分类号： C12N15/09 , C12N9/50 , C12N15/10 , C12Q1/37 , C12Q1/68 , C12Q1/70
CPC分类号： C12N9/506 , C12N15/1048 , C12Q1/37 , C12Q1/6811 , G01N2333/16 , G01N2333/8142 , Y10S435/974 , Y10S435/975
摘要： An in vitro method for predicting the identity of distinct, first-generation, drug-resistant, biologically-active, HIV protease mutants that may emerge in vivo in response to a drug targeted thereagainst. In a preferred embodiment, the in vitro method comprises the steps of (a) preparing, in the presence of the drug, a comprehensive library of all first-generation mutants of the protease differing therefrom by at least one and preferably no more than three amino acid substitutions, each of the protease mutants being generated as part of a polyprotein with the HIV reverse transcriptase protein; (b) isolating, in vitro, first-generation, drug-resistant, biologically-active, mutant proteases from said library by assaying for biological activity of the reverse transcriptase protein; and (c) identifying the distinct, first-generation, biologically-active, mutant proteases so isolated. The present invention also relates to an in vitro method for evaluating the efficacy of a drug against a biologically-active mutant or wild-type form of HIV protease, said method comprising the steps of (a) providing a mutant polyprotein, said mutant polyprotein including a biologically-inactive mutant form of the protease linked to HIV reverse transcriptase by one or more sites cleavable by the biologically-active or wild-type form of the protease; (b) adding the drug to the mutant polyprotein; (c) then, adding the biologically-active or wild-type form of the protease to the mutant polyprotein; and (d) then, assaying for the presence of biological activity for reverse transcriptase, whereby the presence of reverse transcriptase activity indicates that the drug is not efficacious against the biologically-active mutant or wild-type form of the protease tested. The present invention further relates to a kit for evaluating the efficacy of a drug against a biologically-active mutant or wild-type form of HIV protease.

10. 发明授权

US5766842A In vitro method for predicting the evolutionary response of a protein to a drug targeted thereagainst 失效
标题翻译：用于预测蛋白质对其靶向药物的进化反应的体外方法
公开(公告)号：US5766842A
公开(公告)日：1998-06-16
申请号：US706178
申请日：1996-08-30
申请人： Laurence M. Melnick , Donald L. Heefner
发明人： Laurence M. Melnick , Donald L. Heefner
IPC分类号： C12N9/50 , C12N15/10 , C12Q1/37 , C12Q1/68 , C12N15/48 , C12Q1/70
CPC分类号： C12N15/1072 , C12N15/1048 , C12N9/506 , C12Q1/37 , C12Q1/6811 , G01N2333/16 , G01N2333/8142
摘要： A method for identifying, in vitro, distinct, drug-resistant, biologically-active mutants of a protein that may emerge in vivo in response to a drug targeted against the protein is disclosed. The method involves preparing, by heterologous expression of a library of nucleotide sequences, a complete library of mutant proteins accessible in a single generation. The mutant proteins from the library that are drug resistant are identified. When all the first generation mutants have been identified in the above manner, a combination of drugs can be identified that will block the development of resistance. The same technique allows evaluation of the ultimate clinical efficacy of a drug targeted against the protein by comparing the number of resistant first generation mutants. A preferred protein is an HIV protease.
摘要翻译：公开了一种用于鉴定体内可鉴定的针对蛋白质靶向药物可能在体内出现的蛋白质的体外，不同的耐药性，生物活性突变体的方法。该方法包括通过异源表达核苷酸序列文库来制备在单代中可获得的突变蛋白的完整文库。鉴定出抗药性的文库突变蛋白。当所有第一代突变体都以上述方式鉴定时，可以鉴定出将阻止抗性发展的药物组合。相同的技术允许通过比较抗性第一代突变体的数量来评估靶向蛋白质的药物的最终临床疗效。优选的蛋白质是HIV蛋白酶。

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