公开(公告)号：EP0875578A3

公开(公告)日：1999-05-12

申请号：EP98200530.8

申请日：1992-03-18

申请人： ELI LILLY AND COMPANY

发明人： Blaszczak, Larry Chris ,  Skatrud, Paul Luther ,  Smith, Michele Ceceil ,  Wu, Chyun-Yey Earnest

IPC分类号： C12N15/57 ,  C12N9/52 ,  C12N15/62 ,  C07K19/00

CPC分类号： C12N9/52 ,  C07K14/31 ,  C07K2319/00 ,  C07K2319/02 ,  C12N15/625

摘要： The invention provides a gene encoding a novel PBP2A penicillin binding protein isolated from the methicillin resistant S . aureus strain 27R. The invention further provides soluble forms of PBP2A proteins lacking the transmembrane association region yet retain their active site configuration of the PBP2A protein. The invention also provides a method of assaying for agents useful against methicillin resistant staphylococcus strains by creating a kinetically inert complex between a support-immobilized transition metal ion and a modified soluble form of the PBP2A protein incorporating a chelating agent. The invention further provides a cell free method of assaying for agents which bind the PBP2A-27R protein.

公开(公告)号：EP0505151A3

公开(公告)日：1993-04-07

申请号：EP92302298.2

申请日：1992-03-18

申请人： ELI LILLY AND COMPANY

发明人： Blaszczak, Larry Chris ,  Skatrud, Paul Luther ,  Smith, Michele Ceceil ,  Wu, Chyun-Yeh Earnest

IPC分类号： C12N15/57 ,  C12N15/31 ,  C12N15/62 ,  C12N9/52 ,  C07K3/18 ,  C12Q1/37 ,  B01J20/32

CPC分类号： C12N9/52 ,  C07K14/31 ,  C07K2319/00 ,  C07K2319/02 ,  C12N15/625

摘要： The invention provides a gene encoding a novel PBP2A penicillin binding protein isolated from the methicillin resistant S. aureus strain 27R. The invention further provides soluble forms of PBP2A proteins lacking the transmembrane association region yet retain their active site configuration of the PBP2A protein. The invention also provides a method of assaying for agents useful against methicillin resistant staphylococcus strains by creating a kinetically inert complex between a support-mobilized transition metal ion and a modified soluble form of the PBP2A protein incorporating a chelating agent. The invention further provides a cell free method of assaying for agents which bind the PBP2A-27R protein.

公开(公告)号：EP0359540A2

公开(公告)日：1990-03-21

申请号：EP89309281.7

申请日：1989-09-13

申请人： ELI LILLY AND COMPANY

发明人： Blaszczak, Larry Chris

IPC分类号： C07D463/00 ,  C07D501/14 ,  C07D205/085

CPC分类号： C07D205/085 ,  C07D463/04 ,  C07D463/06

摘要： The invention provides a free radical process for preparing 1-carba(1-dethia)cephalosporin antibiotics with 2-substituted methylcephalosporin 1,1-­dioxides wherein the substituent on the 2-methylene group is a free radical precursor group such as a phenyl or alkylseleno group. The latter dioxides are treated with a free radical initiator, e.g., a trialkyl­tin hydride or actinic radiation at 40°C to 150°C to provide the 1-carba-3-cephem and 1-carba-2-cephem products. The invention also provides free radical compounds formed as intermediates in the process.

摘要翻译： 本发明提供了一种用2-取代的甲基头孢菌素1,1-二氧化物制备1-咔（1-脱硫）头孢菌素抗生素的自由基方法，其中2-亚甲基上的取代基是自由基前体基团，例如苯基或烷基硒 组。 后者的二氧化物用自由基引发剂例如氢化三烷基锡或光化辐射在40℃至150℃下处理，得到1-咔唑-3-头孢烯和1-咔二-2-头孢烯产物。 本发明还提供了在该方法中形成为中间体的自由基化合物。

公开(公告)号：EP0163452A1

公开(公告)日：1985-12-04

申请号：EP85303383.5

申请日：1985-05-14

申请人： ELI LILLY AND COMPANY

发明人： Blaszczak, Larry Chris

IPC分类号： C07D205/08

CPC分类号： C07F7/2212 ,  C07D205/085 ,  C07D205/095 ,  C07D477/24 ,  C07F7/10 ,  Y02P20/55

摘要： The invention emcompasses a process for stereoselective carbon-carbon bond formation at the C-4 position of a 3 -(acylamino) azetidinone. The process is carried out under free radical conditions using a (2-substituted or unsubstituted allyl) tin reagent.

摘要翻译： 本发明包括这样的用于在3-（酰氨基）氮杂环丁酮的C-4位的立体选择性碳 - 碳键形成的过程。 该方法使用（2- substituiertem奥德unsubstituiertem烯丙基）锡试剂自由基的条件下进行。

公开(公告)号：EP0122155A2

公开(公告)日：1984-10-17

申请号：EP84302457.1

申请日：1984-04-11

申请人： ELI LILLY AND COMPANY

发明人： Cooper, Robin David Grey ,  Blaszczak, Larry Chris ,  Turner, Jan Ross ,  Conrad, Preston Charles ,  Daugheriy, Byron Wade

IPC分类号： C07D501/20 ,  A61K31/545

CPC分类号： C07D501/20

摘要： Naphthylglycyl and tetrahydronaphthylglycyl cephalosporins are potent antibacterial agents and particularly useful in the oral treatment of upper respiratory infections.

摘要翻译： 萘乙糖基和四氢萘乙糖基头孢菌素是有效的抗菌剂，特别适用于口服上呼吸道感染。

公开(公告)号：EP0122154A2

公开(公告)日：1984-10-17

申请号：EP84302456.3

申请日：1984-04-11

申请人： ELI LILLY AND COMPANY

发明人： Blaszczak, Larry Chris ,  Kukolja, Stjepan ,  Turner, Jan Ross

IPC分类号： C07D501/20 ,  A61K31/545

CPC分类号： C07D333/56 ,  C07D333/60

摘要： 7-(3-Benzothienyl)glycylamido cephalosporins provided by this invention possess favorable pharmacokinetics and are orally-effective against gram positive microorganisms.

公开(公告)号：EP0037729B1

公开(公告)日：1984-01-25

申请号：EP81301479.2

申请日：1981-04-06

申请人： ELI LILLY AND COMPANY

发明人： Blaszczak, Larry Chris

IPC分类号： C07D499/04

CPC分类号： C07D499/00 ,  Y02P20/55

公开(公告)号：EP0672656A1

公开(公告)日：1995-09-20

申请号：EP95301632.6

申请日：1995-03-13

申请人： ELI LILLY AND COMPANY

发明人： Aikins, James Abraham ,  Blaszczak, Larry Chris ,  Lund, Kevin Patrick ,  Rizzo, John Robert

IPC分类号： C07D205/095 ,  C07D471/04

CPC分类号： C07D471/04 ,  C07D205/085 ,  C07D205/095 ,  C07D487/04 ,  Y02P20/55

摘要： The invention provides 1,3,4 substituted and bicyclic derivatives of 2-azetidinones of the formula

wherein R is an amino group, a protected amino group, or a group of the formula -NR a R b , wherein R a is an amino protecting group and R b is selected from the group consisting of acryloyl or substituted acryloyl; R¹ is hydrogen or an amide protecting group; R² is a radical forming group; A is -S- or -(SO) n -, wherein n is 0 or 1; and B and C are independently selected from a group consisting of oxygen, sulfur, methylene, selenium, and nitrogen.
These compounds are valuable intermediates useful in the preparation of 1-carba(dethia)cephalosporin antibiotics.

摘要翻译： 本发明提供了1,3,4- substituiertem和的公式的2-氮杂环丁酮衍生物的双环worin R是氨基，保护的氨基，或下式基团-NR 的R的 worin R a是氨基保护基，R的是选自丙烯酰基或丙烯酰基substituiertem的选择; [R <1>是氢或酰胺保护基团; [R <2>是形成自由基的基团; A为-S-或 - （SO）N-，worin n是0或1; 和B和Cunabhängig从包括氧，硫，亚甲基，硒和氮的组。 这些化合物的1-卡巴（去硫）头孢菌素抗菌素的制备中有用的有价值的中间体。