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1. 发明授权

US3992388A 4-(2-Pyridylamidoethyl)piperidines 失效
标题翻译： 4-（2-吡啶基酰氨基乙基）哌啶
公开(公告)号：US3992388A
公开(公告)日：1976-11-16
申请号：US623351
申请日：1975-10-17
申请人： Wayne E. Barth , Donald E. Kuhla
发明人： Wayne E. Barth , Donald E. Kuhla
IPC分类号： A61K31/445 , C07D213/82 , C07D401/12 , C07D213/56
CPC分类号： C07D213/82 , A61K31/445 , C07D401/12 , Y10S514/866
摘要： Disclosed herein is an improved process for the preparation of known hypoglycemic piperidinesulfamylureas of the structue ##SPC1##Wherein R is selected from the group consisting of 3-(2-methoxy)pyridyl, 3-(2-ethoxy)pyridyl and 2-(4-chloro)pyridyl and R' is selected from the group consisting of bicyclo[2.2.1]hept-5-en-2-yl-endo-methyl, bicyclo[2.2.1]hept-2-yl-endo-methyl, 7-oxabicyclo[2.2.1]hept-2-yl-methyl, 1-adamantyl and cycloalkyl having from five to eight carbon atoms.Said process comprises contacting 4-(2-pyridyl-amidoethyl) piperidine of the structue ##SPC2##With substantially one equivalent of sulfamide thereby exclusively sulfonating the piperidine nitrogen atom. Said 4-(2-pyridylamidoethyl)piperidines from the corresponding 4-(2-pyridylamidoethyl) pyridines by selectively activating the more basic nitrogen atom of said pyridine compound either by N-alkylation or by contact with acid and then exclusively reducing the activated pyridine ring with either hydrogen alone or in combination with a metal hydride. Said 4-(2-pyridylamidoethyl)pyridines are produced by contacting 4-(2-aminoethyl)pyridine with a pyridyl acid chloride of the formula R(C=O)Cl. The piperidine sulfonamides produced by the process of the instant invention are converted to the desired hypoglycemic agent by methods well-known to those skilled in the art.The 4-(2-pyridylamidoethyl)pyridines and piperidines of the instant invention are themselves novel compounds useful as intermediates in the synthesis of piperidine sulfamylurea hypoglycemic agents.
摘要翻译：本文公开了一种用于制备结构+ q，10的已知低血糖哌啶磺酰甲基脲的改进方法，其中R选自3-（2-甲氧基）吡啶基，3-（2-乙氧基）吡啶基和2-（ 4-氯）吡啶基和R'选自双环[2.2.1]庚-5-烯-2-基 - 内 - 甲基，双环[2.2.1]庚-2-基 - 内 - 甲基，7-氧杂二环[2.2.1]庚-2-基 - 甲基，1-金刚烷基和具有5-8个碳原子的环烷基。

2. 发明授权

US3933830A Process for the synthesis of 4-(2-pyridylamido ethyl) piperidines 失效
标题翻译：合成4-（2-吡啶基酰氨基乙基）哌啶的方法
公开(公告)号：US3933830A
公开(公告)日：1976-01-20
申请号：US504826
申请日：1974-09-10
申请人： Wayne E. Barth , Donald E. Kuhla
发明人： Wayne E. Barth , Donald E. Kuhla
IPC分类号： A61K31/445 , C07D213/82 , C07D401/12 , C07D211/02
CPC分类号： C07D213/82 , A61K31/445 , C07D401/12 , Y10S514/866
摘要： Disclosed herein is an improved process for the preparation of known hypoglycemic piperidinesulfamylureas of the structure ##EQU1## wherein R is selected from the group consisting of 3-(2-methoxy)pyridyl, 3-(2-ethoxy)pyridyl and 2-(4-chloro)pyridyl and R' is selected from the group consisting of bicyclo[2.2.1]hept-5-en-2-yl-endo-methyl, bicyclo[2.2.1]hept-2-yl-endo-methyl, 7-oxabicyclo[2.2.1]hept-2-yl-methyl, 1-adamantyl and cycloalkyl having from five to eight carbon atoms.Said process comprises contacting 4-(2-pyridyl-amidoethyl) piperidine of the structure ##EQU2## with substantially one equivalent of sulfamide thereby exclusively sulfonating the piperidine nitrogen atom. Said 4-(2-pyridylamidoethyl)piperidines from the corresponding 4-(2-pyridylamidoethyl) pyridines by selectively activating the more basic nitrogen atom of said pyridine compound either by N-alkylation or by contact with acid and then exclusively reducing the activated pyridine ring with either hydrogen alone or in combination with a metal hydride. Said 4-(2-pyridylamidoethyl)pyridines are produced by contacting 4-(2-aminoethyl)pyridine with a pyridyl acid chloride of the formula R(C=O)Cl. The piperidine sulfonamides produced by the process of the instant invention are converted to the desired hypoglycemic agent by methods well-known to those skilled in the art.The 4-(2-pyridylamidoethyl)pyridines and piperidines of the instant invention are themselves novel compounds useful as intermediates in the synthesis of piperidine sulfamylurea hypoglycemic agents.
摘要翻译：本文公开了一种改进的制备以下结构的已知降血糖哌啶磺酰胺的制备方法：OO PARALLEL PARALLEL R-CNH（CH 2）2 -SO 2 NHC-NHR'，其中R选自3-（2-甲氧基）吡啶基，3 - （2-乙氧基）吡啶基和2-（4-氯）吡啶基，R'选自双环[2.2.1]庚-5-烯-2-基 - 内 - 甲基，双环[2.2。 1]庚-2-基 - 内 - 甲基，7-氧杂双环[2.2.1]庚-2-基 - 甲基，1-金刚烷基和具有5-8个碳原子的环烷基。

3. 发明授权

US4536393A 6-(Aminomethyl)penicillanic acid 1,1-dioxide esters and intermediates therefor 失效
标题翻译： 6-（氨基甲基）青霉烷酸1,1-二氧化物酯及其中间体
公开(公告)号：US4536393A
公开(公告)日：1985-08-20
申请号：US577478
申请日：1984-02-06
申请人： Wayne E. Barth
发明人： Wayne E. Barth
IPC分类号： A61K31/43 , C07D307/88 , C07D499/00 , A61K31/425
CPC分类号： C07D307/88 , C07D499/00
摘要： 6-alpha- and 6-beta-(Aminomethyl)penicillanic acid, 1,1-dioxide esters which are hydrolyzable under physiological conditions, particularly those wherein the ester radical is 1H-isobenzofuran-3-on-1-yl or (5-methyl-1,3-dioxol-2-on-4-yl)methyl, and an improved process and intermediates used in their synthesis.
摘要翻译： 6-α-和6-β-（氨基甲基）青霉烷酸，在生理条件下可水解的1,1-二氧化物酯，特别是其中酯基为1H-异苯并呋喃-3-基-1-基或（5- 甲基-1,3-二氧杂环戊烯-2-基-4-基）甲基，以及用于其合成的改进方法和中间体。

4. 发明授权

US4241050A Penam 1,1-dioxides as beta-lactamase inhibitors 失效
标题翻译： Penam 1,1-二氧化物作为β-内酰胺酶抑制剂
公开(公告)号：US4241050A
公开(公告)日：1980-12-23
申请号：US938848
申请日：1978-09-01
申请人： Wayne E. Barth
发明人： Wayne E. Barth
IPC分类号： C07D499/87 , A61K31/425 , A61K31/43 , A61P31/04 , C07D205/09 , C07D499/00 , C07D499/86 , C07D499/897 , C07D277/60
CPC分类号： C07D205/09 , C07D499/00 , Y02P20/55
摘要： (3S, 5R)-Penam-3-carboxylic acid 1,1-dioxide, optionally having a methyl group at the 2-position, and esters thereof readily hydrolyzable in vivo, are useful for enhancing the effectiveness of several beta-lactam antibiotics against many beta-lactamase producing bacteria.
摘要翻译：（3S，5R） - 可以在2位具有甲基的β-氨基甲酸1,1-二氧化物及其在体内容易水解的酯可用于增强几种β-内酰胺抗生素对抗许多β-内酰胺酶生产细菌。

5. 发明授权

US4179511A Antibacterial 3-(5-tetrazolyl) penam compounds 失效
公开(公告)号：US4179511A
公开(公告)日：1979-12-18
申请号：US957197
申请日：1978-11-01
申请人： Wayne E. Barth
发明人： Wayne E. Barth
IPC分类号： C07D499/00 , A61K31/43
CPC分类号： C07D499/00 , Y02P20/55
摘要： Certain novel 6-acylamino-2,2-dimethyl-3-(5-tetrazolyl)penam derivatives, and salts thereof; their use as broad-spectrum antibacterial agents; and methods for their preparation. Their preparation comprises acylation of the novel intermediate, 6-amino-2,2-dimethyl-3-(5-tetrazolyl)penam or simple derivatives thereof, followed, in some cases, by further transformations of the 6-acylamino group or by removal of a protecting group from the 5-tetrazolyl moiety. Process for the preparation of 6-amino-2,2-dimethyl-3-(5-tetrazolyl)penam, simple derivatives thereof and intermediates therefor.

6. 发明授权

US4113942A 4-(Tetrazol-5-yl)-.DELTA..sup.3 -cephem compounds 失效
标题翻译： 4-（TETRAZOL-5-YL） - “”3“-CEPHEM化合物
公开(公告)号：US4113942A
公开(公告)日：1978-09-12
申请号：US791537
申请日：1977-04-27
申请人： Wayne E. Barth
发明人： Wayne E. Barth
IPC分类号： C07D501/00 , C07D501/18 , C07D501/36
CPC分类号： C07D501/36 , C07D501/00 , C07D501/16 , C07D501/18
摘要： Certain novel antibacterial 7-acylamino-3-substituted-4-(tetrazol-5-yl)-.DELTA..sup.3 -cephem derivatives, and salts thereof, and intermediates useful in their preparation.
摘要翻译：某些新型抗菌7-酰基氨基-3-取代-4-（四唑-5-基）-Δt3 3-头孢烯衍生物及其盐，以及可用于其制备的中间体。

7. 发明授权

US4036846A 3-Hydroxy and 3-acetoxy-6-triphenyl-methylaminopenams 失效
标题翻译： 3-羟基和3-乙酰氧基-6-三苯基 - 甲基氨基戊二酸
公开(公告)号：US4036846A
公开(公告)日：1977-07-19
申请号：US736811
申请日：1976-10-29
申请人： Wayne E. Barth
发明人： Wayne E. Barth
IPC分类号： A23K1/16 , C07D277/10 , C07D499/00 , C07F9/6561
CPC分类号： C07F9/65611 , A23K20/116 , A23K20/137 , C07D277/10 , C07D499/00
摘要： The present invention discloses novel 6-acylamino-2,2-dimethyl-3-phosphonopenams and certain lower alkyl esters thereof possessing antibacterial activity, methods for their production, and intermediates therefor; the production comprises the steps of reacting 6-triphenylmethylamino-2,2-dimethylpenam-3-carboxylic acid with lead tetraacetate to form the corresponding 3-acetoxy compound, the latter is converted to .alpha.-triphenylmethylamino-5,5-dimethyl-3-thiazoline-2-acetic acid which is condensed with dimethyl phosphite to produce .alpha.-triphenylmethylamino-5,5-dimethyl-4(0,0-dimethylphosphono)-thiazolidine-2-acetic acid which is cyclized to 6-triphenylmethylamino-2,2-dimethyl-3-(0,0-dimethylphosphono)penam and the latter is subsequently deblocked and acylated.
摘要翻译：本发明公开了具有抗菌活性的新颖的6-酰基氨基-2,2-二甲基-3-膦草丁酸及其某些低级烷基酯，其生产方法及其中间体; 该制备包括使6-三苯基甲基氨基-2,2-二甲基联苯-3-羧酸与四乙酸铅反应形成相应的3-乙酰氧基化合物的步骤，将其转化成α-三苯甲基氨基-5,5-二甲基-3- 与亚磷酸二甲酯缩合以产生α-三苯基甲基氨基-5,5-二甲基-4（0,0-二甲基膦酰基） - 噻唑烷-2-炔酸的4-噻唑啉-2-乙酸，将其环化为6-三苯基甲基氨基-2， 2-二甲基-3-（0,0-二甲基膦酰基）半缩醛，后者随后被去封闭并酰化。

8. 发明授权

US5270331A Prodrugs of antiinflammatory 3-acyl-2-oxindole-1-carboxamides 失效
标题翻译：抗炎3-酰基-2-羟基吲哚-1-甲酰胺的前药
公开(公告)号：US5270331A
公开(公告)日：1993-12-14
申请号：US009188
申请日：1993-01-26
申请人： Wayne E. Barth , Kelvin Cooper , Edward F. Kleinman , Lawrence A. Reiter , Ralph P. Robinson
发明人： Wayne E. Barth , Kelvin Cooper , Edward F. Kleinman , Lawrence A. Reiter , Ralph P. Robinson
IPC分类号： A61K31/40 , A61K31/404 , A61K31/4433 , A61K31/445 , A61K31/465 , A61K31/535 , A61K31/55 , A61P25/04 , A61P29/00 , A61P43/00 , C07D209/04 , C07D405/00 , C07D409/06 , C07D409/14 , C07F7/18 , C07D403/06
CPC分类号： C07D409/06 , C07D409/14 , C07F7/1856
摘要： Antiinflammatory and analgesic oxindole prodrugs of the formula ##STR1## wherein R.sup.10, R.sup.11, R.sup.12 and R.sup.13 are hydrogen, alkyl or halogen and R is methyleneoxyalkanoyl, methyleneoxyalkenoyl or alkenoyl.
摘要翻译：其中R10，R11，R12和R13为氢，烷基或卤素，R为亚烷基氧基烷酰基，亚甲基氧代烯酰基或烯酰基的抗炎和镇痛羟吲哚前药。

9. 发明授权

US4868296A 6-(1-carbamoyl-1-hydroxymethyl) penicillanic acid derivatives 失效
标题翻译： 6-（1-氨基甲酰基-1-羟甲基）青霉烷酸衍生物
公开(公告)号：US4868296A
公开(公告)日：1989-09-19
申请号：US243568
申请日：1988-09-12
申请人： Wayne E. Barth
发明人： Wayne E. Barth
IPC分类号： C07D499/00 , C07D499/86
CPC分类号： C07D499/00
摘要： 6-(1-Carbamoyl-1-hydroxymethyl)penicillanic acid derivatives are useful as antibacterials and/or beta-lactamase inhibitors.
摘要翻译： 6-（1-氨基甲酰基-1-羟甲基）青霉烷酸衍生物可用作抗菌剂和/或β-内酰胺酶抑制剂。

10. 发明授权

US4797394A 6-(1-carbamoyl-1-hydroxymethyl)penicillanic acid derivatives 失效
标题翻译： 6-（1-氨基甲酰基-1-羟甲基）青霉烷酸衍生物
公开(公告)号：US4797394A
公开(公告)日：1989-01-10
申请号：US85675
申请日：1987-06-05
申请人： Wayne E. Barth
发明人： Wayne E. Barth
IPC分类号： C07D499/00 , A61K31/425
CPC分类号： C07D499/00
摘要： 6-(1-Carbamoyl-1-hydroxymethyl)penicillanic acid derivatives are useful as antibacterials and/or beta-lactamase inhibitors.
摘要翻译： PCT No.PCT / US85 / 02134 Sec。 371日期：1987年6月5日 102（e）1987年6月5日PCT 1985年10月29日PCT。6-（1-氨甲酰基-1-羟甲基）青霉烷酸衍生物可用作抗菌剂和/或β-内酰胺酶抑制剂。

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