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1. 发明授权

US4704385A 3-formamido azetidinone antibacterial agents, their preparation and use 失效
标题翻译： 3-甲酰氨基氮杂环丁酮抗菌剂，其制备和用途
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.

2. 发明授权

US4940702A Cephem compounds 失效
标题翻译：头孢烯化合物
公开(公告)号：US4940702A
公开(公告)日：1990-07-10
申请号：US894926
申请日：1986-08-08
申请人： Stephen C. Finch , Michael J. Pearson
发明人： Stephen C. Finch , Michael J. Pearson
IPC分类号： A61K31/545 , C07D20060101 , C07D501/00 , C07D501/22 , C07D501/57 , C07D519/00
CPC分类号： C07D501/57
摘要： .beta.-Lactam antibiotics are disclosed which have the formulae (Ia) or pharmaceutically acceptable salts or pharmaceutically acceptable in vivo hydrolysable esters thereof: ##STR1## wherein R.sup.1 is phenyl, substituted phenyl, cyclohexenyl, cyclohexadienyl, or an optionally substituted 5- or 6-membered heterocyclic ring containing up to three hetero-atoms selected from oxygen, sulphur or nitrogen; R.sup.2 is hydrogen or optionally substituted C.sub.1-6 alkyl; R.sup.3 is an optionally substituted 5- or 6- membered heterocyclic group containing one or two nitrogen heteroatoms; or R.sup.2 and R.sup.3 together with the nitrogen atom to which they are attached form an optionally substituted 5- or 6- membered heterocyclic group contaning one or two nitrogen heteroatoms; R.sup.4 is a substituted pyridinium group; and CO.sub.2 R is carboxy or a carboxylate anion; and also the use thereof.Processes for the preparation of the compounds are disclosed together with intermediates for use therein.
摘要翻译：公开了具有式（Ia）或其药学上可接受的盐或其药学上可接受的体内可水解的酯的β-内酰胺抗生素：其中R1是苯基，取代的苯基，环己烯基，环己二烯基或任选取代的5- 或含有至多三个选自氧，硫或氮的杂原子的6元杂环; R2是氢或任选取代的C 1-6烷基; R3是任选取代的含有一个或两个氮杂原子的5-或6-元杂环基; 或R 2和R 3与它们所连接的氮原子一起形成任选取代的含有一个或两个氮杂原子的5-或6-元杂环基; R4是取代的吡啶鎓基; 和CO 2 R是羧基或羧酸根阴离子; 以及其使用。公开了用于制备化合物的方法以及用于其中的中间体。

3. 发明授权

US4678782A 3S-formamido azetidinone antibacterial agents, their preparation and use 失效
标题翻译： 3S-甲酰氨基氮杂环丁酮抗菌剂，其制备和应用
公开(公告)号：US4678782A
公开(公告)日：1987-07-07
申请号：US679574
申请日：1984-12-07
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 , A61K31/495
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 substitutent 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.

4. 发明授权

US4647558A Antibacterial agents, their preparation and use 失效
标题翻译：抗菌剂，其制备和用途
公开(公告)号：US4647558A
公开(公告)日：1987-03-03
申请号：US459675
申请日：1983-01-20
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.
摘要翻译：包括在3S位具有甲酰氨基取代基的单环β-内酰胺抗生素，包括式（I）的化合物：其中R是-SO 3 H; -PO（OH）Y，其中Y为C 1-6烷氧基，羟基，芳氧基，C 1-6烷基或芳基; 其中Z代表C1-6烷基或芳基; 其中Z 1和Z 2可以相同或不同，各自表示氢，C 1-6烷基，芳基，氨基或C 1-6烷氧基，或者Z 1和Z 2一起形成杂环的残基; -OSO3H; 或，其中X是氢或羟基; R1是氨基，保护的氨基或羧基酰基氨基，R2和R3独立地选自氢或1至18个碳原子的烃基。

5. 发明授权

US5316998A HCl adsorbent and method for making and using same 失效
标题翻译： HCl吸附剂及其制备和使用方法
公开(公告)号：US5316998A
公开(公告)日：1994-05-31
申请号：US878857
申请日：1992-05-05
申请人： John S. Lee , Michael J. Pearson
发明人： John S. Lee , Michael J. Pearson
IPC分类号： B01D53/04 , B01D53/68 , B01J20/04 , B01J20/08 , C01B7/01 , C01B7/00
CPC分类号： B01J20/08 , B01D53/68 , B01J20/041 , B01J20/28011 , B01J20/28069 , B01J20/28078 , B01J20/3078 , B01J20/3204 , B01J20/3236 , C01B7/01
摘要： An HCl adsorbent, and method of making and using the adsorbent, the adsorbent comprising an activated alumina promoted with an alkali metal in an amount such that if calculated as alkali metal oxide, the adsorbent contains at least about 5% by weight alkali metal oxide.
摘要翻译： HCl吸附剂，以及制造和使用吸附剂的方法，所述吸附剂包含用碱金属促进的活性氧化铝，其量使得如果以碱金属氧化物计算，则吸附剂含有至少约5重量％的碱金属氧化物。

6. 发明授权

US4252808A .beta.-Lactam antibacterial agents, their use in pharmaceutical compositions, the process for their preparation and intermediates for use in that process 失效
标题翻译： β-内酰胺抗菌剂，它们在药物组合物中的应用，其制备方法和用于该方法的中间体
公开(公告)号：US4252808A
公开(公告)日：1981-02-24
申请号：US15006
申请日：1979-02-26
申请人： Michael J. Pearson
发明人： Michael J. Pearson
IPC分类号： A61K31/505 , A61P31/04 , C07D205/085 , C07D205/095 , C07D487/14
CPC分类号： C07D487/14 , A61K31/505 , C07D205/085 , C07D205/095
摘要： The compounds of the formula (I): ##STR1## wherein R.sup.1 is a hydrogen atom, a trityl group or an acyl group as found in known antibacterially active penicillins or cephalosporins; R.sup.2 is a hydrogen atom, a lower alkyl group or an aryl group; R.sup.3 is a hydrogen atom, a lower alkyl group, a substituted lower alkyl or a thiosubstituted lower alkyl group; and R.sup.4 is a group such that CO.sub.2 R.sup.4 is a carboxylic acid group or a salt or readily removable ester thereof; are antibiotics. The compounds may be formulated in pharmaceutical compositions.Processes for the preparation of the compounds (I) are also described.
摘要翻译：式（I）的化合物：其中R 1是氢原子，三苯甲基或酰基，如在已知的抗菌活性青霉素或头孢菌素中所发现的; R2是氢原子，低级烷基或芳基; R3是氢原子，低级烷基，取代的低级烷基或取代的低级烷基; 并且R 4是这样的基团，使得CO 2 R 4是羧酸基团或其盐或易于除去的酯; 是抗生素。化合物可以配制成药物组合物。还描述了制备化合物（I）的方法。

7. 发明授权

US4918067A Heterocyclic substituted penicillin antibiotics 失效
标题翻译：杂环取代青霉素抗生素
公开(公告)号：US4918067A
公开(公告)日：1990-04-17
申请号：US76360
申请日：1987-07-22
申请人： Brian C. Gasson , Michael J. Pearson
发明人： Brian C. Gasson , Michael J. Pearson
IPC分类号： C07D499/00 , C07D499/70
CPC分类号： C07D499/00
摘要： The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt or in-vivo hydrolysable ester thereof: ##STR1## wherein R.sup.1 is a 5 or 6 membered sulphur and/or nitrogen containing heterocyclic group substituted by an optionally protected amino group, with the proviso that R.sup.1 is not 2-aminothiazol-4-yl, and R is hydrogen; optionally substituted C.sub.1-12 alkyl; optionally substituted C.sub.2-12 alkenyl or alkynyl; carbocyclyl; aryl or heterocyclyl.These compounds have antibacterial properties, and therefore are of use in the treatment of bacterial infections in humans and animals caused by a wide range of organizations.
摘要翻译：本发明提供式（I）化合物或其药学上可接受的盐或体内可水解的酯：其中R 1是被任选地被取代的5或6元硫和/或含氮杂环基团保护的氨基，条件是R1不是2-氨基噻唑-4-基，R是氢; 任选取代的C 1-12烷基; 任选取代的C 12-12烯基或炔基; 碳环基芳基或杂环基。这些化合物具有抗菌性，因此可用于治疗由广泛组织引起的人和动物细菌感染。

8. 发明授权

US4868147A Alumina of high macroporosity and stability 失效
标题翻译：氧化铝具有高的大孔性和稳定性
公开(公告)号：US4868147A
公开(公告)日：1989-09-19
申请号：US177233
申请日：1988-04-01
申请人： Michael J. Pearson , William A. Belding
发明人： Michael J. Pearson , William A. Belding
IPC分类号： B01J20/08 , B01J21/04 , B01J21/12 , B01J35/10 , B01J37/26
CPC分类号： B01J21/12 , B01J20/08 , B01J21/04 , B01J35/002 , B01J35/1009 , B01J35/1014 , B01J35/1042 , B01J35/1057 , B01J37/26
摘要： A calcined and shaped alumina, exhibiting a stabilized, high pore volume and a low surace area together with high strength, is made from an alumina, such as pseudoboehmite or chi-rho-eta alumina or mixtures of different alumina species. The stabilized product exhibits a total porosity of at least about 0.4 cc/g, a surface area within the range of about 2-20 m.sup.2 /g. The porosity is stabilized by treatment of the alumina, prior to calcination, with a combination of silica and an inorganic fluoride. The stabilized alumina product can be readily utilized as an adsorbent or a catalyst support, particularly in applications where the catalyst is subjected to high temperatures.
摘要翻译：煅烧和成型的氧化铝由氧化铝，例如假勃姆石或氯化堇或氧化铝或不同氧化铝物质的混合物制成，具有稳定的，高孔体积和低外观面积以及高强度。稳定的产品表现出至少约0.4cc / g的总孔隙率，表面积在约2-20m 2 / g的范围内。通过在煅烧之前用二氧化硅和无机氟化物的组合处理氧化铝来稳定孔隙率。稳定的氧化铝产品可以容易地用作吸附剂或催化剂载体，特别是在催化剂经受高温的应用中。

9. 发明授权

US4639259A Promoted scavenger for purifying HCl-contaminated gases 失效
标题翻译：促进清除剂净化HCl污染的气体
公开(公告)号：US4639259A
公开(公告)日：1987-01-27
申请号：US785706
申请日：1985-10-09
申请人： Michael J. Pearson
发明人： Michael J. Pearson
IPC分类号： B01D53/02 , B01D53/14 , B01D53/68 , B01J20/04 , B01J20/08 , C10G25/00 , C10K1/32 , C10K1/34 , B01D53/04
CPC分类号： B01D53/02 , B01D53/68 , B01J20/08
摘要： HCl-contaminated gas streams are purified by contacting the contaminated gas with an alumina-containing material which has been promoted with an alkaline earth metal salt.
摘要翻译：通过使受污染的气体与用碱土金属盐促进的含氧化铝材料接触来净化HCl污染的气流。

10. 发明授权

US4444771A Azeto triazolo pyrazine .beta.-lactam antibacterial agents 失效
标题翻译： Azeto三唑并吡唑β-内酰胺抗菌剂
公开(公告)号：US4444771A
公开(公告)日：1984-04-24
申请号：US299629
申请日：1981-09-04
申请人： Michael J. Pearson , Clive L. Branch
发明人： Michael J. Pearson , Clive L. Branch
IPC分类号： A61K31/495 , A61P31/04 , C07D205/085 , C07D487/14 , C07F7/08 , C07D205/08 , C07D403/06
CPC分类号： C07D487/14 , C07D205/085 , C07F7/0812 , Y02P20/55
摘要： A compound of formula (I) or a salt thereof: ##STR1## wherein R.sup.1 is an amino group, an azido group, or an acylamino group as found in antibacterially active penicillins or cephalosporins;R.sup.2 is a hydrogen atom or a C.sub.1-4 alkyl group;R.sup.3 is a hydrogen atom, or a C.sub.1-4 alkyl group optionally substituted by a carboxyl, carboxylic ester, hydroxy, C.sub.1-4 alkyloxy, acyloxy or heterocyclylthio group; andR.sup.4 is hydrogen or a readily removable carboxyl protecting group.The compounds wherein R.sup.1 is an acylamino group are found in known antibacterially active penicillins and cephalosporins and wherein R.sup.4 is a hydrogen, a pharmaceutically acceptable salting ion or an in vivo hydrolyzable ester forming radical may be formulated in pharmaceutical compositions.Processes for the preparation of the compound (I) are also described.
摘要翻译：式（I）化合物或其盐：其中R1是抗菌活性青霉素或头孢菌素中发现的氨基，叠氮基或酰氨基; R2是氢原子或C1-4烷基; R3是氢原子或任选被羧基，羧酸酯，羟基，C 1-4烷氧基，酰氧基或杂环硫基取代的C 1-4烷基; R4为氢或易除去的羧基保护基。在已知的抗菌活性青霉素和头孢菌素中发现其中R 1是酰氨基的化合物，其中R 4是氢，可药用的盐析离子或体内可水解的酯形成基团的化合物可以配制在药物组合物中。还描述了制备化合物（I）的方法。

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