专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明授权

US4271173A 6-Amino-spiro[penam-2,4'-piperidine]-3-carboxylic acid, antibacterial compositions thereof and method of use thereof 失效
标题翻译： 6-氨基螺[penam-2,4'-哌啶] -3-羧酸，其抗菌组合物及其使用方法
公开(公告)号：US4271173A
公开(公告)日：1981-06-02
申请号：US162615
申请日：1980-06-24
申请人： Ludovic Rodriguez , Jacques Leclercq , Pierre Ykman , Eric Cossement
发明人： Ludovic Rodriguez , Jacques Leclercq , Pierre Ykman , Eric Cossement
IPC分类号： C07D499/46 , A61K31/43 , A61K31/431 , A61P31/04 , C07D499/00 , C07D499/64 , C07D499/68 , C07D499/74 , C07D499/76 , C07D499/80 , C07D499/90 , C07D499/32 , A61K31/425
CPC分类号： C07D499/00
摘要： 6-Amino-spiro[penam-2,4'-piperidine]-3-carboxylic acid derivatives having the formula ##STR1## wherein R is a methyl, phenyl or benzyl radical, Z.sub.1 is a hydrogen atom and Z.sub.2 is a radical selected from those known from penicillin chemistry and is preferably a 2-phenylacetyl, 2-amino-2-phenylacetyl, 5-methyl-3-phenyl-4-isoxazolecarbonyl or 2,6-dimethoxybenzoyl radical, or Z.sub.1 and Z.sub.2 together represent a bivalent radical Z.sub.3 and preferably a (hexahydro-1H-azepin-1-yl)methylene radical, as well as the pharmaceutically acceptable non-toxic salts thereof and process for preparing the same.These compounds have valuable antibacterial properties and are useful as therapeutic agents in the treatment of infectious diseases caused by Gram-positive and Gram-negative bacteria.
摘要翻译： 6-氨基螺[penam-2,4'-哌啶] -3-羧酸衍生物，其结构式为：其中R为甲基，苯基或苄基，Z1为氢原子，Z2为选自由青霉素化学已知的那些，优选2-苯基乙酰基，2-氨基-2-苯基乙酰基，5-甲基-3-苯基-4-异恶唑羰基或2,6-二甲氧基苯甲酰基，或Z 1和Z 2一起代表二价基团Z 3 并且优选为（六氢-1H-吖庚因-1-基）亚甲基，以及其药学上可接受的无毒盐及其制备方法。这些化合物具有有价值的抗菌性质，可用作治疗由革兰氏阳性菌和革兰氏阴性菌引起的传染病的治疗剂。

2. 发明授权

US4139628A Amino-spiro[oxa(or thia)cycloalkane-penam]-carboxylic acid derivatives 失效
标题翻译：氨基螺（8）氧杂（或硫杂）环烷烃 - penam {9-羧酸衍生物
公开(公告)号：US4139628A
公开(公告)日：1979-02-13
申请号：US869860
申请日：1978-01-16
申请人： Ludovic Rodriguez , Jacques Leclercq , Pierre Ykman , Eric Cossement
发明人： Ludovic Rodriguez , Jacques Leclercq , Pierre Ykman , Eric Cossement
IPC分类号： C07D513/20 , A61K31/43 , A61K31/431 , A61P31/04 , C07D499/00 , C07D499/21 , C07D499/44 , C07D499/90
CPC分类号： C07D499/00
摘要： Amino-spiro[oxa(or thia)cycloalkane-penam]-carboxylic acid derivatives having the formula ##STR1## WHEREIN X is a sulfur or oxygen atom or the sulfinyl group, n is 1 or 2, m is 1 or 2, R.sub.1 is hydrogen, R.sub.2 is one of the radicals known in the chemistry of the penicillins, preferably 2-phenylacetyl, 2-amino-2-phenylacetyl, 5-methyl-3-phenyl-4-isoxazolecarbonyl or 2,6-dimethoxybenzoyl, or R.sub.1 and R.sub.2 together represent a bivalent radical R.sub.3, preferably (hexahydro-1H-azepin-1-yl)methylene and their therapeutically acceptable non-toxic salts and process for preparing the same.These compounds have valuable antibacterial properties and are useful as therapeutic agents in the treatment of infectious diseases caused by Gram-positive and Gram-negative bacteria.
摘要翻译：具有式“IMAGE”的X'（或硫杂）环烷烃 - penam] - 羧酸衍生物，X为硫或氧原子或亚磺酰基，n为1或2，m为1或2，R 1为氢，R2是青霉素化学中已知的基团之一，优选2-苯乙酰基，2-氨基-2-苯乙酰基，5-甲基-3-苯基-4-异恶唑羰基或2,6-二甲氧基苯甲酰基，或R1和 R2一起代表二价基团R 3，优选（六氢-1H-吖庚因-1-基）亚甲基及其治疗上可接受的无毒盐及其制备方法。

3. 发明授权

US4271172A 6-Amino-spiro[penam-2,4'-piperidine]-3-carboxylic acids, antibacterial compositions thereof and method of use thereof 失效
标题翻译： 6-氨基螺[penam-2,4'-哌啶] -3-羧酸，其抗菌组合物及其使用方法
公开(公告)号：US4271172A
公开(公告)日：1981-06-02
申请号：US162616
申请日：1980-06-24
申请人： Ludovic Rodriguez , Jacques Leclercq , Pierre Ykman , Eric Cossement
发明人： Ludovic Rodriguez , Jacques Leclercq , Pierre Ykman , Eric Cossement
IPC分类号： C07D499/06 , A61K31/43 , A61K31/431 , A61P31/04 , C07D499/00 , C07D499/18 , C07D499/42 , C07D499/90 , C07D513/10 , C07D499/76 , C07D499/58 , C07D499/74
CPC分类号： C07D513/10 , C07D499/00
摘要： 6-Amino-spiro[penam-2,4'-piperidine]-3-carboxylic acids, salts and esters thereof of the formula ##STR1## wherein R.sub.1 is hydrogen, benzyl or an alkali metal or ammonium ion and R.sub.2 is methyl, phenyl or benzyl and process for preparing the same.These compounds are useful as intermediates in the synthesis of a new group of antibiotics having properties similar to penicillins, besides own antibiotic activity with a broad antibacterial spectrum. Therefore, they are useful as antibacterials agents and as therapeutic agents for humans and for animals in the treatment of infectious diseases caused by Gram-positive and Gram-negative bacteria.
摘要翻译： 6-氨基螺[penam-2,4'-哌啶] -3-羧酸，其盐及其酯，其中R 1是氢，苄基或碱金属或铵离子，R 2是甲基，苯基或苄基及其制备方法。这些化合物可用作合成具有与青霉素类似的性质的新一组抗生素的中间体，除了具有广泛抗菌谱的自身抗生素活性外。因此，它们作为抗菌剂和作为人和动物的治疗剂用于治疗由革兰氏阳性和革兰氏阴性菌引起的感染性疾病。

4. 发明授权

US4137236A Amino-spiro[oxa(or thia)cycloalkane-penam]-carboxylic 失效
标题翻译：氨基螺（8）氧杂（或硫杂）环烷烃 - penam {9-羧酸
公开(公告)号：US4137236A
公开(公告)日：1979-01-30
申请号：US869859
申请日：1978-01-16
申请人： Ludovic Rodriguez , Jacques Leclerca , Pierre Ykman , Eric Cossement
发明人： Ludovic Rodriguez , Jacques Leclerca , Pierre Ykman , Eric Cossement
IPC分类号： C07D513/20 , A61K31/431 , A61P31/04 , C07D305/08 , C07D307/18 , C07D309/08 , C07D309/20 , C07D331/04 , C07D333/34 , C07D335/02 , C07D499/00 , C07D499/04 , C07D499/42 , C07D499/44 , C07D499/90 , C07D513/10 , C07D277/04
CPC分类号： C07D307/18 , C07D305/08 , C07D309/08 , C07D309/20 , C07D331/04 , C07D333/34 , C07D335/02 , C07D499/00 , C07D513/10
摘要： Amino-spiro[oxa(or thia)cycloalkane-penam]-carboxylic acid, a salt or an ester thereof, of the formula ##STR1## wherein Z is a hydrogen or an alkali metal atom, or a group protecting the carboxylic function, X is a sulfur or oxygen atom, n is 1 or 2, m is 1 or 2, and process of preparing the same.These compounds are useful as intermediates in the synthesis of a new group of antibiotics having properties similar to penicillins, besides own antibiotic activity with a broad antibacterial spectrum.
摘要翻译：或者其中Z为氢或碱金属原子的式（Ⅰ）的氨基螺[氧杂（或硫杂）环烷烃 - 半脒] - 羧酸，其盐或酯，或保护羧酸功能，X为硫原子或氧原子，n为1或2，m为1或2，以及其制备方法。

5. 发明授权

US4145343A 6'-Amino-spiro�cycloalkane-1,2'-penam!-3'-carboxylic acid derivatives 失效
标题翻译： 6“-AMINO-SPIRO（CYCLOALKANE-1,2”-PENAM）-3“ - 羧酸衍生物
公开(公告)号：US4145343A
公开(公告)日：1979-03-20
申请号：US800083
申请日：1977-05-24
申请人： Ludovic Rodriguez , Jacques Leclercq
发明人： Ludovic Rodriguez , Jacques Leclercq
IPC分类号： A61K31/43 , A61P31/04 , C07D499/00 , C07D499/44 , C07D499/90
CPC分类号： C07D499/00
摘要： 6'-Amino-spiro�cycloalkane-1,2'-penam!-3'-carboxylic acid derivatives having the formula ##STR1## WHEREIN N IS A WHOLE NUMBER OF FROM 3 TO 6 AND R.sub.1 and R.sub.2 represent substituents known in the chemistry of penicillins, and their pharmaceutically acceptable, non-toxic salts, have valuable antibacterial properties and are useful as therapeutic agents in the treatment of infectious diseases caused by Gram-positive and Gram-negative bacteria. Processes for preparing these compounds are also described.

6. 发明授权

US4091027A 6'-Amino-spiro(cycloalkane-1,2'-penam)-3'-carboxylic acids 失效
标题翻译： 6 {40-氨基螺（环烷-1,1 {40-对氨基）-3 {40-羧酸
公开(公告)号：US4091027A
公开(公告)日：1978-05-23
申请号：US800082
申请日：1977-05-24
申请人： Ludovic Rodriguez , Jacques Leclercq
发明人： Ludovic Rodriguez , Jacques Leclercq
IPC分类号： C07D277/60 , C07D499/00 , C07D499/42
CPC分类号： C07D277/60 , C07D499/00 , Y02P20/55
摘要： 6'-Amino-spiro[cycloalkane-1,2'-penam]-3'-carboxylic acids of the formula ##STR1## WHEREIN Z is a hydrogen or an alkali metal atom, or a protective group, and n a whole number of from 3 to 6, and process of preparing the same.These compounds are useful as intermediates in the synthesis of a new group of antibiotics having properties similar to the penicillins.
摘要翻译：式“IMAGE”的6'-氨基螺[环烷-1,2'-半胱氨酸] -3'-羧酸，其中Z是氢或碱金属原子，或保护基，并且na整数 3〜6及其制备方法。

7. 发明授权

US4443460A 2-[4-(Diphenylmethylene)-1-piperidinyl]-acetic acids and their amides 失效
标题翻译： 2- [4-（二苯基亚甲基）-1-哌啶基] - 乙酸及其酰胺
公开(公告)号：US4443460A
公开(公告)日：1984-04-17
申请号：US303522
申请日：1981-09-17
申请人： Ludovic Rodriguez , Eugene Baltes
发明人： Ludovic Rodriguez , Eugene Baltes
IPC分类号： A61K31/445 , A61K31/451 , A61K31/452 , A61P11/00 , A61P11/08 , A61P25/20 , A61P37/08 , A61P43/00 , C07D211/70 , C07D211/22
CPC分类号： C07D211/70 , Y10S514/816 , Y10S514/826
摘要： New 2-[4-(diphenylmethylene)-1-piperidinyl]-acetic acids and their amides, processes for the preparation thereof and therapeutic compositions. These compounds have the formula ##STR1## wherein Y=--OH or --NR.sub.1 R.sub.2, R.sub.1 and R.sub.2 =H, alkyl or phenyl; X=H, halogen or alkoxy; m=0, 1 or 2 and n=1 or 2.The 2-[4-(diphenylmethylene)-1-piperidinyl]-acetic acids are prepared by hydrolyzing the corresponding amide or lower alkyl ester, whereas the amides are prepared either by reacting a 4-(diphenylmethylene)-piperidine with an omega-haloacetamide, or by reacting an alkali metal salt of an omega-[4-diphenylmethylene)-1-piperidinyl]-alkanol (m=1 or 2) with a 2-haloacetamide, or by reacting a nitrogen compound (HNR.sub.1 R.sub.2) with a halide or alkyl ester of a 2-[4-(diphenylmethylene)-1-piperidinyl]-acetic acid.These compounds have in particular an antiallergic, spasmolytic, antihistaminic and broncholytic activity.
摘要翻译：新的2- [4-（二苯基亚甲基）-1-哌啶基] - 乙酸及其酰胺，其制备方法和治疗组合物。这些化合物具有其中Y = -OH或-NR1R2，R1和R2 = H，烷基或苯基的式“IMAGE” X = H，卤素或烷氧基; m = 0,1或2，n = 1或2.通过水解相应的酰胺或低级烷基酯制备2- [4-（二苯基亚甲基）-1-哌啶基] - 乙酸，而酰胺由使4-（二苯基亚甲基） - 哌啶与ω-卤代乙酰胺反应，或通过使ω-[4-二苯基亚甲基] -1-哌啶基] - 烷醇（m = 1或2）的碱金属盐与2-卤代乙酰胺或通过使氮化合物（HNR1R2）与2- [4-（二苯基亚甲基）-1-哌啶基] - 乙酸的卤化物或烷基酯反应。这些化合物特别具有抗过敏，解痉，抗组胺和支气管分解活性。

8. 发明授权

US4221789A Lactam-N-acetic acids and their amides 失效
标题翻译：内酰胺-N-乙酸及其酰胺
公开(公告)号：US4221789A
公开(公告)日：1980-09-09
申请号：US036987
申请日：1979-05-07
申请人： Ludovic Rodriguez , Lucien Marchal
发明人： Ludovic Rodriguez , Lucien Marchal
IPC分类号： C07D207/28 , A61K31/341 , A61K31/40 , A61K31/4015 , A61K31/4025 , A61K31/4355 , A61K31/443 , A61K31/445 , A61K31/451 , A61K31/4523 , A61K31/495 , A61K31/535 , A61P9/00 , A61P9/04 , A61P25/00 , A61P25/28 , C07D207/26 , C07D207/27 , C07D211/70 , C07D211/76 , C07D223/10 , C07D227/08 , C07D403/06 , C07D405/04 , C07D405/12 , A61K31/395 , C07D207/12 , C07D401/06
CPC分类号： C07D207/27 , A61K31/40 , A61K31/445 , C07D207/26 , C07D211/76 , C07D223/10 , C07D227/08
摘要： New lactam-N-acetic acids and amides thereof having the formula ##STR1## wherein R.sub.1 and R.sub.2 =H, C.sub.1 -C.sub.4 -alkyl, aryl or halogen-substituted aryl,R.sub.3 =OH or --NR.sub.4 R.sub.5,R.sub.4 and R.sub.5 =H, C.sub.1 -C.sub.4 -alkyl, cycloalkyl, aralkyl or, taken together with the N atom form alkyleneimino, oxa-alkyleneimino, aza-alkyleneimino or N-benzyl-aza-alkyleneimino,m is 3, 4 or 5, preferably 3,n is 0, 1 or 2, preferably 2;and the pharmaceutically acceptable salts of said acids. Processes for producing these compounds and pharmaceutical compositions containing the same are also given. These compounds show amongst others beneficial activity on the mnemic processes and cardiac activity.
摘要翻译：其中R 1和R 2 = H，C 1 -C 4烷基，芳基或卤素取代的芳基，R 3 = OH或-NR 4 R 5，R 4和R 5 = H，C 1 -C 4烷基，芳基或卤素取代的芳基的新的内酰胺-N-乙酸及其酰胺 -C 1-4 - 烷基，环烷基，芳烷基或与N原子一起形成亚烷基亚氨基，氧杂 - 亚烷基亚氨基，氮杂 - 亚烷基亚氨基或N-苄基 - 氮杂 - 亚烷基亚氨基，m为3,4或5，优选3，n为0， 1或2，优选2; 和所述酸的药学上可接受的盐。还给出了制备这些化合物的方法和含有它们的药物组合物。这些化合物显示了有益于活动过程和心脏活动的活性。

9. 发明授权

US4525358A 2-[4-(Diphenylmethyl)-1-piperazinyl]-acetic acids and their amides 失效
标题翻译： 2- [4-（二苯基甲基）-1-哌嗪基] - 乙酸及其酰胺
公开(公告)号：US4525358A
公开(公告)日：1985-06-25
申请号：US496489
申请日：1983-05-17
申请人： Eugene Baltes , Jean de Lannoy , Ludovic Rodriguez
发明人： Eugene Baltes , Jean de Lannoy , Ludovic Rodriguez
IPC分类号： C07D295/08 , A61K31/495 , A61P37/08 , C07D295/088 , A61K31/50 , C07D295/14
CPC分类号： C07D295/088
摘要： New 2-[4-(diphenylmethyl)-1-piperazinyl]-acetic acids, their amides and their salts, processes for the preparation thereof and therapeutic compositions. These compounds have the formula ##STR1## wherein Y=--OH or --NH.sub.2 ; X and X'=H, halogen, alkoxy or trifluoromethyl; m=1 or 2 and n=1 or 2.The amides of the 2-[4-(diphenylmethyl)-1-piperazinyl]-acetic acids are prepared either by reacting a 1-(diphenylmethyl)-piperazine with an omegahaloacetamide, or by reacting an alkali metal salt of an omega-[4-(diphenylmethyl)-1-piperazinyl]-alkanol with a 2-haloacetamide, or yet by reacting ammonia with a halide or alkyl ester of a 2-[4-(diphenylmethyl)-1-piperazinyl]-acetic acid, whereas the 2-[4-(diphenylmethyl)-1-piperazinyl]-acetic acids are prepared by hydrolyzing the corresponding amide or lower alkyl ester.These compounds have in particular an antiallergic, spasmolytic and antihistaminic activity.
摘要翻译：新的2- [4-（二苯基甲基）-1-哌嗪基] - 乙酸，它们的酰胺及其盐，其制备方法和治疗组合物。这些化合物具有其中Y = -OH或-NH 2的式“IMAGE”; X和X'= H，卤素，烷氧基或三氟甲基; m = 1或2，n = 1或2. 2- [4-（二苯基甲基）-1-哌嗪基] - 乙酸的酰胺通过1-（二苯基甲基） - 哌嗪与ω加酰胺乙酰胺或通过使ω-[4-（二苯基甲基）-1-哌嗪基] - 烷醇的碱金属盐与2-卤代乙酰胺反应，或者通过使氨与2- [4-（二苯基甲基） -1-哌嗪基] - 乙酸，而2- [4-（二苯基甲基）-1-哌嗪基] - 乙酸通过水解相应的酰胺或低级烷基酯来制备。这些化合物特别具有抗过敏，解痉和抗组胺活性。

10. 发明授权

US4162325A N-substituted lactams 失效
标题翻译： N-取代的内酰胺
公开(公告)号：US4162325A
公开(公告)日：1979-07-24
申请号：US843692
申请日：1977-10-19
申请人： Ludovic Rodriguez , Lucien Marchal
发明人： Ludovic Rodriguez , Lucien Marchal
IPC分类号： C07D201/02 , A61K31/40 , A61K31/4015 , A61K31/435 , A61K31/55 , A61P7/00 , A61P7/06 , A61P9/00 , A61P9/04 , A61P25/24 , A61P25/28 , C07D207/26 , C07D207/27 , C07D211/76 , C07D223/10 , C07K1/113 , C07K5/06
CPC分类号： C07D207/27 , C07D223/10
摘要： New physiologically active N-substituted lactams having the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6 and R.sub.7, represent independently a hydrogen atom, an alkyl radical containing 1 to 4 carbon atoms or a phenyl group, R.sub.8 is a hydrogen atom or R.sub.8 and R.sub.3 together form the ethylene or trimethylene radical, and n is 3, 4 or 5, processes for the preparation thereof and pharmaceutical compositions containing the same.
摘要翻译：具有式“IMAGE”的新的生理活性N-取代的内酰胺，其中R1，R2，R3，R4，R5，R6和R7独立地表示氢原子，含有1-4个碳原子的烷基或苯基，R8是氢原子或R8和R3一起形成乙烯或三亚甲基，n为3,4或5，其制备方法和含有它们的药物组合物。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式