公开(公告)号：US4518606A

公开(公告)日：1985-05-21

申请号：US396711

申请日：1982-07-09

Applicant: Edmond Saias

Inventor： Edmond Saias

IPC: A61M5/178 ,  A61K9/00 ,  A61K31/43 ,  A61K47/10 ,  A61P31/04 ,  C07D499/64 ,  C07D499/68 ,  C07D499/86 ,  C07D499/87 ,  C07D499/897

CPC classification number: A61K47/10 ,  A61K31/43 ,  A61K9/0019

Abstract: A pharmaceutical composition for injection which comprises an aqueous sterile solution of a penicillin or salt thereof and from 1 to 10% of benzyl alcohol, a two-pack container or two-part syringe wherein one pack or part contains a penicillin or salt thereof in the form of a dry powder and the second pack or part contains an aqueous solution of benzyl alcohol, such that mixing the contents of the two packs or parts produces an aqueous solution of the penicillin and from 1 to 10% of benzyl alcohol, and a two-pack container or two-part syringe wherein one pack or part contains a penicillin in a solid free acid form, and the second part contains an aqueous solution of benzyl alcohol and substantially one equivalent of a basic pharmaceutically acceptable salt, such that mixing the contents of the two packs or parts produces an aqueous solution of a salt of the penicillin and from 1 to 10% of benzyl alcohol.

Abstract translation: 一种用于注射的药物组合物，其包含青霉素或其盐的无水水溶液和1至10％的苄醇，双组分容器或两部分注射器，其中一个包装或一部分含有青霉素或其盐 形式的干粉，第二包或部分含有苄醇水溶液，使得混合两个包装或部分的内容物产生青霉素的水溶液和1至10％的苄醇，并且将二 包装容器或两部分注射器，其中一个包装或一部分含有固体游离酸形式的青霉素，第二部分含有苯甲醇的水溶液和基本上1当量的碱性药学上可接受的盐，使得将内容物 的两个或多个组分产生青霉素的盐水溶液和1至10％的苄醇。

公开(公告)号：US4505894A

公开(公告)日：1985-03-19

申请号：US412591

申请日：1982-08-30

Applicant: Roger J. Ponsford

Inventor： Roger J. Ponsford

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

CPC classification number: A61K31/43 ,  A61K31/545 ,  C07D503/00

Abstract: 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.

Abstract translation: 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：US4490383A

公开(公告)日：1984-12-25

申请号：US448240

申请日：1982-12-09

Applicant: Stuart A. Hill

Inventor： Stuart A. Hill

IPC: A61K9/08 ,  A61K9/00 ,  A61K31/43 ,  A61K47/02

CPC classification number: A61K9/0019 ,  A61K31/43 ,  A61K47/02

Abstract: A pharmaceutical composition adapted for administration to a human by injection which composition comprises an aqueous solution containing sodium amoxycillin and tri-sodium phosphate, the weight ratio of sodium amoxycillin present to the tri-sodium phosphate present being from 8:1 to 50:1.

Abstract translation: 适于通过注射给予人的药物组合物，该组合物包含含有阿莫西林钠和三磷酸钠的水溶液，存在的阿莫西林钠与三磷酸钠的重量比为8:1至50:1。

公开(公告)号：US4481209A

公开(公告)日：1984-11-06

申请号：US204845

申请日：1980-11-07

Applicant: Kenneth Utting ,  Karrar A. Khan ,  Sidney E. Callander

Inventor： Kenneth Utting ,  Karrar A. Khan ,  Sidney E. Callander

IPC: C07D501/02 ,  C07D499/00 ,  C07D499/68 ,  A61K31/43 ,  C07D499/32

CPC classification number: C07D499/00

Abstract: Ampicillin phthalidyl ester naphthalene-2-sulphonate, its preparation, and its use in pharmaceutical compositions to treat infections.

Abstract translation: 氨苄青霉素酞酸酯萘-2-磺酸盐，其制备及其在药物组合物中的用途，用于治疗感染。

公开(公告)号：US4473578A

公开(公告)日：1984-09-25

申请号：US403076

申请日：1982-07-29

Applicant: David F. Corbett

Inventor： David F. Corbett

IPC: C07D477/20 ,  A61K31/395 ,  C07D487/04

CPC classification number: C07D477/20

Abstract: The compounds of the formula: ##STR1## and pharmaceutically acceptable salts and in-vivo hydrolysable esters thereof wherein R.sup.1 is a hydrogen atom or a group selected from OH, OSO.sub.3 H or a pharmaceutically acceptable salt or C.sub.1-4 alkyl ester thereof, OR.sup.2, SR.sup.3, OCOR.sup.2, OCO.sub.2 R.sup.3 or OCONHR.sup.3, where R.sup.2 is a C.sub.1-6 alkyl group or an optionally substituted benzyl group and R.sup.3 is a C.sub.1-6 alkyl group or an optionally substituted benzyl or an optionally substituted phenyl group; and R.sup.22 is a hydrogen atom, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.3-6 alkynyl wherein the triple bond is not present on the carbon adjacent to the sulphur atom, aralkyl, C.sub.1-6 alkanoyl, aralkanoyl, aryloxyalkanoyl or arylcarbonyl, any of such R.sup.22 groups being optionally substituted; with the proviso that when R.sup.22 is 2-aminoethyl R.sup.1 must be SR.sup.3 or OSO.sub.3 H or a pharmaceutically acceptable salt of C.sub.1-4 alkyl ester thereof; have been found to be antibacterially active. Their use is described as are processes for their preparation.

Abstract translation: 下式的化合物及其药学上可接受的盐和体内可水解的酯，其中R1是氢原子或选自OH，OSO3H或其药学上可接受的盐或C 1-4烷基的基团，OR 2，SR 3 ，OCOR 2，OCO 2 R 3或OCONHR 3，其中R 2是C 1-6烷基或任选取代的苄基，R 3是C 1-6烷基或任选取代的苄基或任选取代的苯基; R 22为氢原子，C 1-6烷基，C 2-6烯基，C 3-6炔基，其中三元键不存在于与硫原子相邻的碳上，芳烷基，C 1-6烷酰基，芳烷酰基，芳氧基烷酰基或芳基羰基， 任何这样的R22基团任选被取代; 条件是当R 22是2-氨基乙基时，R 1必须是SR 3或OSO 3 H或其药学上可接受的盐的C 1-4烷基酯; 已被发现具有抗菌活性。 它们的使用被描述为它们的制备方法。

公开(公告)号：US4465689A

公开(公告)日：1984-08-14

申请号：US115364

申请日：1979-01-25

Applicant: Kong Luk ,  John P. Clayton ,  Norman H. Rogers

Inventor： Kong Luk ,  John P. Clayton ,  Norman H. Rogers

IPC: A61K31/335 ,  A61K31/35 ,  A61K31/435 ,  A61P31/04 ,  C07D309/10 ,  C07D407/06

CPC classification number: A61K31/435 ,  C07D407/06

Abstract: Esters of an acid of formula: ##STR1## which is termed "monic acid" have activity against Gram-positive and Gram-negative organisms.

Abstract translation: 被称为“单酸”的下式的酸：的酸具有抗革兰氏阳性和革兰氏阴性生物的活性。

公开(公告)号：US4454069A

公开(公告)日：1984-06-12

申请号：US334438

申请日：1981-12-24

Applicant: Michael A. Cook ,  Alan D. Curzons ,  Robert B. Wilkins

Inventor： Michael A. Cook ,  Alan D. Curzons ,  Robert B. Wilkins

IPC: C07D503/00 ,  C07D498/04

CPC classification number: C07D503/00

Abstract: This invention provides a novel process for the preparation of clavulanic acid and pharmaceutically acceptable salts and esters thereof which process utilizes the preparation of the tertiary-butylamine salt of clavulanic acid optionally in the form of an acetone solvate and subsequently converting said salt into the desired product.

Abstract translation: 本发明提供了一种用于制备克拉维酸及其药学上可接受的盐和酯的新方法，该方法利用任选地以丙酮溶剂化物的形式制备克拉维酸的叔丁胺盐，随后将所述盐转化为所需产物 。

公开(公告)号：US4446069A

公开(公告)日：1984-05-01

申请号：US269897

申请日：1981-06-03

Applicant: Kong Luk

Inventor： Kong Luk

IPC: A61K31/43 ,  A61P31/04 ,  C07D499/00 ,  C07D499/86 ,  C07D499/87 ,  C07D499/897 ,  C07D503/00 ,  C07D501/04

CPC classification number: C07D503/00 ,  C07D499/00

Abstract: The present invention provides a process for the preparation of a fused bicyclic .beta.-lactam containing compound having an optionally salified free carboxylic acid group which process comprises the reaction of an ester of the formula (I): ##STR1## with halide ion; wherein R is the residue of the fused bicyclic .beta.-lactam containing compound, R.sup.1 is an alkyl group of 1-6 carbon atoms optionally substituted by an alkoxy group of 1-4 carbon atoms or is an optionally substituted phenyl group or an alkyl group of 1-4 carbon atoms substituted by an optionally substituted phenyl group; and R.sup.2 is a hydrogen atom or an alkyl group of 1-4 carbon atoms or is joined to R.sup.2 to form part of a 5- or 6- membered carbocyclic or heterocyclic ring.

Abstract translation: 本发明提供制备含有任选盐化游离羧酸基团的稠合双环β-内酰胺化合物的方法，该方法包括式（I）的酯与卤离子的反应 ; 其中R是含有稠合双环β-内酰胺的化合物的残基，R1是任选被1-4个碳原子的烷氧基取代的1-6个碳原子的烷基，或者是任选取代的苯基或烷基 1-4个碳原子被任选取代的苯基取代; 并且R 2是氢原子或1-4个碳原子的烷基，或者与R 2连接形成5-或6-元碳环或杂环的一部分。

公开(公告)号：US4442098A

公开(公告)日：1984-04-10

申请号：US332347

申请日：1981-12-18

Applicant: Derek V. Gardner ,  Laramie M. Gaster

Inventor： Derek V. Gardner ,  Laramie M. Gaster

IPC: A61K31/55 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  C07D223/20 ,  C07D267/20 ,  C07D471/16 ,  C07D487/04 ,  C07D498/04 ,  C07D498/16 ,  C07D513/04 ,  C07D513/16 ,  C07D471/06 ,  A61K31/495 ,  C07D498/06 ,  C07D513/06

CPC classification number: C07D487/04 ,  C07D223/20 ,  C07D267/20

Abstract: Compounds of formula (I): ##STR1## wherein: X is CH.sub.2, O, S or NR wherein R is hydrogen or C.sub.1-4 alkyl;Y and Z are independently selected from hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halogen or CF.sub.3 ;R.sub.1 is hydrogen, C.sub.1-6 alkyl, phenyl or phenyl-C.sub.1-4 alkyl any of which phenyl moieties may be substituted by one or more of C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halogen or CF.sub.3 ;R.sub.2 is hydrogen, OH, C.sub.1-6 alkoxy, phenyl-C.sub.1-4 alkoxy, C.sub.1-7 acyloxy or NR.sub.4 R.sub.5 wherein R.sub.4 and R.sub.5 are independently selected from hydrogen or C.sub.1-6 alkyl; R.sub.4 is hydrogen and R.sub.5 is OH or C.sub.1-4 alkoxy; or R.sub.4 and R.sub.5 together form C.sub.3-6 polymethylene optionally interrupted by O or NR.sub.6 where R.sub.6 is hydrogen or C.sub.1-4 alkyl; or together with R.sub.1 forms an oxo group or .dbd.NOR.sub.7 wherein R.sub.7 is hydrogen or C.sub.1-6 alkyl; andR.sub.3 is hydrogen or C.sub.1-6 alkyl have useful pharmacological activity, processes for their preparation and their use.

Abstract translation: 式（I）化合物：其中：X为CH 2，O，S或NR，其中R为氢或C 1-4烷基; Y和Z独立地选自氢，C 1-4烷基，C 1-4烷氧基，卤素或CF 3; R 1是氢，C 1-6烷基，苯基或苯基-C 1-4烷基，其中任一个苯基部分可以被一个或多个C 1-6烷基，C 1-6烷氧基，卤素或CF 3取代; R 2是氢，OH，C 1-6烷氧基，苯基-C 1-4烷氧基，C 1-7酰氧基或NR 4 R 5，其中R 4和R 5独立地选自氢或C 1-6烷基; R4是氢，R5是OH或C1-4烷氧基; 或R 4和R 5一起形成任选地被O或NR 6中断的C 3-6的多亚甲基，其中R 6是氢或C 1-4烷基; 或与R 1一起形成氧基或= NOR7，其中R 7为氢或C 1-6烷基; R3为氢或C1-6烷基具有有用的药理活性，其制备方法及其用途。

公开(公告)号：US4438101A

公开(公告)日：1984-03-20

申请号：US944808

申请日：1978-09-22

Applicant: Roger J. Ponsford ,  Thomas T. Howarth

Inventor： Roger J. Ponsford ,  Thomas T. Howarth

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

CPC classification number: A61K31/545 ,  A61K31/43 ,  C07D503/00

Abstract: 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.

Abstract translation: 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。