公开(公告)号：US4505894A

公开(公告)日：1985-03-19

申请号：US412591

申请日：1982-08-30

申请人： Roger J. Ponsford

发明人： Roger J. Ponsford

IPC分类号： C07D503/08 ,  A61K31/42 ,  A61K31/424 ,  A61K31/43 ,  A61K31/545 ,  A61P31/04 ,  C07D503/00 ,  C07D503/20 ,  A61K35/00

CPC分类号： A61K31/43 ,  A61K31/545 ,  C07D503/00

摘要： Compounds of the formula ##STR1## wherein X is S, SO or SO.sub.2 and R is an inert hydrocarbon of up to 20 carbon atoms which will not lead to rapid degradation of the above compound unsubstituted or substituted and A is a group such and CO.sub.2 A represents a carboxylic acid group or a salt or ester thereof, are useful for their antibacterial activity and for their .beta.-lactamase inhibitory activity.

摘要翻译： 式中，X为S，SO或SO 2的化合物，R为至多20个碳原子的惰性烃，其不会导致上述未被取代或取代的化合物的快速降解，A是这样的基团，而CO 2 A表示 羧酸基团或其盐或酯可用于其抗菌活性和β-内酰胺酶抑制活性。

公开(公告)号：US4438101A

公开(公告)日：1984-03-20

申请号：US944808

申请日：1978-09-22

申请人： Roger J. Ponsford ,  Thomas T. Howarth

发明人： Roger J. Ponsford ,  Thomas T. Howarth

IPC分类号： C07D503/06 ,  A61K31/42 ,  A61K31/424 ,  A61K31/43 ,  A61K31/545 ,  A61P31/04 ,  C07D503/00 ,  C07D503/22 ,  A61K35/00

CPC分类号： A61K31/545 ,  A61K31/43 ,  C07D503/00

摘要： The compounds of the formula (II): ##STR1## and salts and esters thereof wherein R.sub.1 is an inert organic group of up to 14 carbon atoms and R.sub.2 is an inert organic group of up to 16 carbon atoms, the group NR.sub.1 R.sub.2 containing up to 22 carbon atoms, are antibacterial agents able to enhance the effectiveness of penicillins and cephalosporins against certain .beta.-lactamase producing bacteria.

摘要翻译： 式（II）化合物：其中R 1为至多14个碳原子的惰性有机基团，R 2为至多16个碳原子的惰性有机基团，NR1R2基团 含有多达22个碳原子的抗菌剂是能够增强青霉素和头孢菌素对某些β-内酰胺酶生产菌的有效性的抗菌剂。

公开(公告)号：US4263314A

公开(公告)日：1981-04-21

申请号：US4891

申请日：1979-01-19

申请人： Roger J. Ponsford ,  Robert Southgate ,  Patricia M. Roberts

发明人： Roger J. Ponsford ,  Robert Southgate ,  Patricia M. Roberts

IPC分类号： C07D477/04 ,  C07D477/20 ,  A61K31/40 ,  C07D487/04

CPC分类号： C07D477/20 ,  C07D477/04

摘要： The present invention provides the antibacterial agents of the formula (II): ##STR1## wherein R.sub.1 is a group such that CO.sub.2 R.sub.1 is a carboxylic acid group or a salt thereof or is a group of the formula CO.sub.2 R.sub.1.sup.1 wherein R.sub.1.sup.1 is a group such that CO.sub.2 R.sub.1.sup.1 is an ester group, R.sub.2 is a hydrogen atom or a lower alkyl group; R.sub.3 is a hydrogen atom or a lower alkyl group; and R.sub.4 is a phenyl group or a phenyl group substituted by one or two groups selected from fluorine, chlorine, OR.sub.5, NH.CO.R.sub.5, NH.CO.sub.2 R.sub.5 or CO.sub.2 R.sub.5 where R.sub.5 is a lower alkyl or benzyl group.A process for their preparation and their use in pharmaceutical compositions is also described.

摘要翻译： 本发明提供式（II）的抗菌剂：其中R 1是CO 2 R 1是羧酸基或其盐的基团，或者是式CO 2 R 11的基团，其中R 11是这样的基团，使得CO 2 R 11 是酯基，R2是氢原子或低级烷基; R3是氢原子或低级烷基; R 4是苯基或被一个或两个选自氟，氯，OR 5，NH.CO.R 5，NH.CO 2 R 5或CO 2 R 5的基团取代的苯基，其中R 5是低级烷基或苄基。 还描述了其制备方法及其在药物组合物中的应用。

公开(公告)号：US5126335A

公开(公告)日：1992-06-30

申请号：US496777

申请日：1990-03-21

申请人： Roger J. Ponsford ,  Andrew V. Stachulski

发明人： Roger J. Ponsford ,  Andrew V. Stachulski

IPC分类号： C07D499/00 ,  C07D499/46

CPC分类号： C07D499/00 ,  Y02P20/55

摘要： Compounds of formula (I) and pharmaceutically acceptable salts and in-vivo hydrolysable esters thereof: ##STR1## wherein X is hydrogen or a group NHR.sup.1, wherein R.sup.1 is hydrogen or an amino protecting group, and R is an optionally substituted 5-membered or 6-membered saturated heterocyclic group containing 1 or 2 heteroatoms selected from oxygen, sulphur or nitrogen, are useful in the treatment of bacterial infections in humans and animals.

公开(公告)号：US4609495A

公开(公告)日：1986-09-02

申请号：US278564

申请日：1981-06-29

申请人： Roger J. Ponsford ,  Thomas T. Howarth

发明人： Roger J. Ponsford ,  Thomas T. Howarth

IPC分类号： A61K31/42 ,  A61K31/43 ,  A61K31/545 ,  C07D503/00 ,  C07D498/04

CPC分类号： A61K31/42 ,  A61K31/43 ,  A61K31/545 ,  C07D503/00

摘要： The compounds of the formula (II): ##STR1## and salts and esters thereof wherein R is an inert organic group of up to 18 carbon atoms and are able to inhibit the action of various bacterial .beta.-lactamases. Thus when a compound of the formula (II) or its salt or ester is used together with a penicillin or cephalosporin, the effectiveness of that penicillin or cephalosporin can be considerably enhanced. These novel synergysts can be prepared by etherification of an ester of clavulanic acid followed if desired by deesterification. The novel synergysts also possess antibacterial activity.

摘要翻译： 式（II）的化合物：其中R是具有至多18个碳原子的惰性有机基团并能够抑制各种细菌β-内酰胺酶的作用的盐和酯。 因此，当将式（II）化合物或其盐或酯与青霉素或头孢菌素一起使用时，可以显着提高该青霉素或头孢菌素的有效性。 这些新型协同增效剂可以通过使用克拉维酸的酯化来制备，如果需要，通过酯化作用。 新型增效剂也具有抗菌活性。

公开(公告)号：US4548815A

公开(公告)日：1985-10-22

申请号：US538767

申请日：1983-10-03

申请人： Roger J. Ponsford ,  Thomas T. Howarth

发明人： Roger J. Ponsford ,  Thomas T. Howarth

IPC分类号： A61K31/42 ,  A61K31/43 ,  A61K31/545 ,  C07D503/00 ,  A61K35/00

CPC分类号： A61K31/42 ,  A61K31/43 ,  A61K31/545 ,  C07D503/00

摘要： The compounds of the formula (II): ##STR1## and salts and esters thereof wherein R is an inert ogranic group of up to 18 carbon atoms and are able to inhibit the action of various bacterial .beta.-lactamases. Thus when a compound of the formula (II) or its salt or ester is used together with a penicillin or cephalosporin, the effectiveness of that penicillin or cephalosporin can be considerably enhanced. These novel synergysts can be prepared by etherification of an ester of clavulanic acid followed if desired by deesterification. The novel synergysts also possess antibacterial activity.

摘要翻译： 式（II）的化合物：其中R是具有至多18个碳原子的惰性极性基团并且能够抑制各种细菌β-内酰胺酶的作用的盐和酯。 因此，当将式（II）化合物或其盐或酯与青霉素或头孢菌素一起使用时，可以显着提高该青霉素或头孢菌素的有效性。 这些新型协同增效剂可以通过使用克拉维酸的酯化来制备，如果需要，通过酯化作用。 新型增效剂也具有抗菌活性。

公开(公告)号：US4245089A

公开(公告)日：1981-01-13

申请号：US6435

申请日：1979-01-25

申请人： Roger J. Ponsford ,  Robert Southgate

发明人： Roger J. Ponsford ,  Robert Southgate

IPC分类号： C07D265/02 ,  C07D498/04 ,  C07D265/12

CPC分类号： C07D265/02

摘要： Compounds of the formula (III): ##STR1## wherein R.sub.1 is alkyl of up to 3 carbon atoms and R.sub.2 is alkyl of up to 3 carbon atoms optionally joined to R.sub.1 so that R.sub.1 and R.sub.2 and the carbon atom to which they are attached form a spiro-cyclopentyl or spiro-cyclohexyl ring, and wherein the configuration about the .beta.-lactam ring is trans, are useful in the preparation of antibacterial .beta.-lactam compounds.A process for the preparation of the compounds of the formula (III), is also desired.

摘要翻译： 式（III）的化合物：其中R 1是至多3个碳原子的烷基，R 2是至多3个碳原子的烷基，其任选地连接到R 1上，使得R 1和R 2及它们的碳原子 连接形成螺 - 环戊基或螺环己基环，并且其中关于β-内酰胺环的构型是反式的，可用于制备抗细菌β-内酰胺化合物。 还需要制备式（III）化合物的方法。

公开(公告)号：US4228174A

公开(公告)日：1980-10-14

申请号：US8421

申请日：1979-02-01

申请人： Roger J. Ponsford ,  Thomas T. Howarth

发明人： Roger J. Ponsford ,  Thomas T. Howarth

IPC分类号： A61K31/42 ,  A61P31/04 ,  C07D503/00 ,  C07D498/04

CPC分类号： C07D503/00

摘要： The compounds of the formula (II): ##STR1## and salts and esters thereof wherein R is an inert organic group of up to 18 carbon atoms and are able to inhibit the action of various bacterial .beta.-lactamases. Thus when a compound of the formula (II) or its salt or ester is used together with a penicillin or cephalosporin, the effectiveness of that penicillin or cephalosporin can be considerably enhanced. These novel synergysts can be prepared by etherification of an ester of clavulanic acid followed if desired by de-esterification. The novel synergysts also possess antibacterial activity.

摘要翻译： 式（II）的化合物：其中R是具有至多18个碳原子的惰性有机基团并能够抑制各种细菌β-内酰胺酶的作用的盐和酯。 因此，当将式（II）化合物或其盐或酯与青霉素或头孢菌素一起使用时，可以显着提高该青霉素或头孢菌素的有效性。 如果需要，通过脱酯化可以通过使克拉维酸的酯化来制备这些新颖的增效剂。 新型增效剂也具有抗菌活性。

公开(公告)号：US4704385A

公开(公告)日：1987-11-03

申请号：US835346

申请日：1986-03-03

申请人： Roger J. Ponsford ,  Michael J. Pearson ,  Stephen C. Finch

发明人： Roger J. Ponsford ,  Michael J. Pearson ,  Stephen C. Finch

IPC分类号： C07D205/08 ,  A61K31/395 ,  A61K31/397 ,  A61K31/425 ,  A61P31/04 ,  C07D205/085 ,  C07D403/04 ,  C07D403/12 ,  C07D409/12 ,  C07D417/12 ,  C07F7/10 ,  C07F7/18 ,  C07F9/568 ,  C07D401/12

CPC分类号： C07D403/04 ,  C07D205/085 ,  C07D403/12 ,  C07D409/12 ,  C07D417/12 ,  C07F7/10 ,  C07F9/5683

摘要： A monocyclic .beta.-lactam antibiotic having a formamido substituent at the 3S-position, including compounds of the formula (I): ##STR1## and salts thereof wherein R is --SO.sub.3 H; --PO(OH)Y wherein Y is C.sub.1-6 alkoxy, hydroxy, aryloxy, C.sub.1-6 alkyl or aryl; ##STR2## wherein Z represents C.sub.1-6 alkyl or aryl; ##STR3## wherein Z.sup.1 and Z.sup.2 may be the same or different and each represents hydrogen, C.sub.1-6 alkyl, aryl, amino or C.sub.1-6 alkoxy, or Z.sup.1 and Z.sup.2 together form the residue of a heterocyclic ring; --OSO.sub.3 H; or ##STR4## where X is hydrogen or hydroxy; R.sup.1 is an amino, protected amino or carboxylic acylamino group, and R.sup.2 and R.sup.3 are independently selected from hydrogen or a hydrocarbon group of 1 to 18 carbon atoms.

公开(公告)号：US4179562A

公开(公告)日：1979-12-18

申请号：US815565

申请日：1977-07-14

申请人： Roger J. Ponsford

发明人： Roger J. Ponsford

IPC分类号： A61K31/505 ,  A61P31/04 ,  C07D239/48

CPC分类号： C07D239/48 ,  Y10S514/895

摘要： Compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof and antimalarial and antibacterial compositions containing an effective amount of active agent and a pharmaceutically acceptable carrier particularly in oral dosage form wherein R is hydrogen, methyl or ethyl; X is alkylene of 1-10 carbon atoms; Y is oxygen, sulphur or a bond, and Ar is an optionally substituted aryl moiety; are useful for their antimalarial and antibacterial activity.

摘要翻译： 式IMA化合物及其药学上可接受的盐和抗疟和抗菌组合物，其特征在于其中R为氢，甲基或乙基，其含有有效量的活性剂和药学上可接受的载体; X是1-10个碳原子的亚烷基; Y是氧，硫或键，Ar是任选取代的芳基部分; 对抗疟疾和抗菌活性有用。