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1. 发明授权

US4101661A Novel antibacterial amide compounds and process means for producing the same 失效
标题翻译：新型抗菌酰胺化合物及其制备方法
公开(公告)号：US4101661A
公开(公告)日：1978-07-18
申请号：US803004
申请日：1977-06-03
申请人： James S. Kaltenbronn , Theodore H. Haskell , Leonard Doub
发明人： James S. Kaltenbronn , Theodore H. Haskell , Leonard Doub
IPC分类号： C07D499/66 , A61K31/44 , A61K31/545 , A61K31/546 , A61P31/04 , C07D211/22 , C07D213/78 , C07D213/80 , C07D213/82 , C07D213/85 , C07D499/00 , C07D499/64 , C07D499/68 , C07D501/20 , C07D501/57 , C07D521/00 , A61K31/43 , A61K31/455
CPC分类号： C07D213/78 , C07D211/22 , C07D213/80 , C07D213/82 , C07D213/85 , C07D231/12 , C07D233/56 , C07D249/08 , C07D499/00
摘要： Novel organic amide compounds which are N-[6-[(aminosulfonyl)phenyl]-1,2-dihydro-2-oxonicotinyl]penicillin and cephalosporin type compounds having broad spectrum antibacterial utility are provided by (a) reacting the free amino acid of the appropriate penicillin or cephalosporin or the acid salt or silylated derivative or complex thereof with a reactive derivative of the corresponing N-6-[(aminosulfonyl)phenyl]-1,2-dihydro-2-oxonicotinic acid or (b) reacting the free amino acid 6-aminopenicillanic acid, 7-aminocephalosporanic acid, 7-amino-3-methylceph-3-em-4-carboxylic acid or a related compound or the acid salt or silylated derivative thereof with a reactive derivative of the corresponding D-N-[6-[(aminosulfonyl)phenyl]-1,2-dihydro-2-oxonicotinyl]-2-substituted glycine. Pharmaceutical compositions containing said compounds and methods for treating infections using said compositions are also disclosed.
摘要翻译：通过以下方法提供了具有广谱抗菌效用的N- [6 - [（氨基磺酰基）苯基] -1,2-二氢-2-氧代烟碱基]青霉素和头孢菌素型化合物的新型有机酰胺化合物：（a）使游离氨基酸适当的青霉素或头孢菌素或其酸盐或甲硅烷基化的衍生物或配合物与对应的N-6 - [（氨基磺酰基）苯基] -1,2-二氢-2-氧代烟酸的反应性衍生物或（b）使游离氨基酸6-氨基青霉烷酸，7-氨基头孢烷酸，7-氨基-3-甲基头孢-3-烯-4-羧酸或其相关化合物或其酸式盐或甲硅烷基化衍生物与相应的DN- [ 6 - [（氨基磺酰基）苯基] -1,2-二氢-2-氧代烟酰基] -2-取代的甘氨酸。还公开了含有所述化合物的药物组合物和使用所述组合物治疗感染的方法。

2. 发明授权

US4137408A [Amino sulfonyl-2-oxo-nicotinyl]derivatives of cephalosporin 失效
标题翻译： {8氨基磺酰基-2-氧代 - 烟酰基{9衍生物的头孢菌素
公开(公告)号：US4137408A
公开(公告)日：1979-01-30
申请号：US845996
申请日：1977-10-27
申请人： James S. Kaltenbronn , Theodore H. Haskell , Leonard Doub
发明人： James S. Kaltenbronn , Theodore H. Haskell , Leonard Doub
IPC分类号： C07D499/66 , A61K31/44 , A61K31/545 , A61K31/546 , A61P31/04 , C07D211/22 , C07D213/78 , C07D213/80 , C07D213/82 , C07D213/85 , C07D499/00 , C07D499/64 , C07D499/68 , C07D501/20 , C07D501/57 , C07D521/00 , C07D501/34
CPC分类号： C07D213/78 , C07D211/22 , C07D213/80 , C07D213/82 , C07D213/85 , C07D231/12 , C07D233/56 , C07D249/08 , C07D499/00
摘要： Novel organic amide compounds which are N-[6-[(aminosulfonyl)phenyl]-1,2-dihydro-2-oxonicotinyl]penicillin and cephalosporin type compounds having broad spectrum antibacterial utility are provided by (a) reacting the free amino acid of the appropriate penicillin or cephalosporin or the acid salt or silylated derivative or complex thereof with a reactive derivative of the corresponding N-6-[(aminosulfonyl)phenyl]-1,2-dihydro-2-oxonicotinic acid or (b) reacting the free amino acid 6-aminopenicillanic acid, 7-aminocephalosporanic acid, 7-amino-3-methylceph-3-em-4-carboxylic acid or a related compound or the acid salt or silylated derivative thereof with a reactive derivative of the corresponding D-N-[6-[(aminosulfonyl)phenyl]-1,2-dihydro-2-oxonicotinyl]-2-substituted glycine. Pharmaceutical compositions containing said compounds and methods for treating infections using said compositions are also disclosed.
摘要翻译：通过以下方法提供了具有广谱抗菌效用的N- [6 - [（氨基磺酰基）苯基] -1,2-二氢-2-氧代烟碱基]青霉素和头孢菌素型化合物的新型有机酰胺化合物：（a）使游离氨基酸适当的青霉素或头孢菌素或其酸盐或甲硅烷基化的衍生物或配合物与相应的N-6 - [（氨基磺酰基）苯基] -1,2-二氢-2-氧代烟酸的反应性衍生物或（b）使游离氨基酸6-氨基青霉烷酸，7-氨基头孢烷酸，7-氨基-3-甲基头孢-3-烯-4-羧酸或其相关化合物或其酸式盐或甲硅烷基化衍生物与相应的DN- [ 6 - [（氨基磺酰基）苯基] -1,2-二氢-2-氧代烟酰基] -2-取代的甘氨酸。还公开了含有所述化合物的药物组合物和使用所述组合物治疗感染的方法。

3. 发明授权

US4053470A Substituted-1,2-dihydro-2-oxonicotinyl-cephalosporins 失效
标题翻译：取代的1,2-二羟基-2-氧代丁基胆碱酯
公开(公告)号：US4053470A
公开(公告)日：1977-10-11
申请号：US650098
申请日：1976-01-19
申请人： Leonard Doub , James S. Kaltenbronn , Dieter Schweiss
发明人： Leonard Doub , James S. Kaltenbronn , Dieter Schweiss
IPC分类号： C07D499/00 , C07D501/20 , A61K31/545 , C07D499/44
CPC分类号： C07D499/00
摘要： Novel organic amide compounds which are N-[6-[(substituted amino)phenyl] 1,2-dihydro-2-oxonicotinyl]penicillin and cephalosporin type compounds having broad spectrum antibacterial utility are provided by (a) reacting the free amino acid of the appropriate penicillin or cephalosporin or the acid salt or silylated derivative thereof with a reactive derivative of the corresponding N-6-[(substituted amino)phenyl]-1,2-dihydro-2-oxonicotinic acid or (b) reacting the free amino acid 6-amino-penicillanic acid, 7-aminocephalosporanic acid, 7-amino-3-methylceph-3-em-4-carboxylic acid or a related compound or the acid salt or silylated derivative thereof with a reactive derivative of the corresponding D-N-[6-[(substituted amino)phenyl]-1,2-dihydro-2-oxonicotinyl]-2-substituted glycine. Pharmaceutical compositions containing said compounds and methods for treating infections using said compositions are also disclosed.

4. 发明授权

US3954734A Novel antibacterial amide compounds and process means for producing the same 失效
标题翻译：新型抗菌酰胺化合物及其制备方法
公开(公告)号：US3954734A
公开(公告)日：1976-05-04
申请号：US534031
申请日：1974-12-23
申请人： Leonard Doub , James S. Kaltenbronn , Dieter Schweiss
发明人： Leonard Doub , James S. Kaltenbronn , Dieter Schweiss
IPC分类号： C07D499/00 , C07D499/64 , C07D499/68 , C07D499/66 , C07D499/70
CPC分类号： C07D499/00
摘要： Novel organic amide compounds which are N-[6-[(substituted amino)phenyl]-1,2-dihydro-2-oxonicotinyl]penicillin and cephalosporin type compounds having broad spectrum antibacterial utility are provided by (a) reacting the free amino acid of the appropriate penicillin or cephalosporin or the acid salt or silylated derivative thereof with a reactive derivative of the corresponding N-6-[(substituted amino)phenyl]-1,2-dihydro-2-oxonicotinic acid or (b) reacting the free amino acid 6-amino-penicillanic acid, 7-aminocephalosporanic acid, 7-amino-3-methylceph-3-em-4-carboxylic acid or a related compound or the acid salt or silylated derivative thereof with a reactive derivative of the corresponding D-N-[6-[(substituted amino)phenyl]-1,2-dihydro-2-oxonicotinyl]-2-substituted glycine. Pharmaceutical compositions containing said compounds and methods for treating infections using said compositions are also disclosed.
摘要翻译：提供了具有广谱抗菌效用的N- [6 - [（取代氨基）苯基] -1,2-二氢-2-氧代烟碱基]青霉素和头孢菌素型化合物的新型有机酰胺化合物是通过（a）使游离氨基酸的适当的青霉素或头孢菌素或其酸性盐或甲硅烷基化衍生物与相应的N-6 - [（取代的氨基）苯基] -1,2-二氢-2-氧代烟酸的反应性衍生物或（b）使游离氨基酸6-氨基 - 青霉烷酸，7-氨基头孢烷酸，7-氨基-3-甲基头孢-3-烯-4-羧酸或其相关化合物或其酸盐或甲硅烷基化衍生物与相应DN的反应性衍生物 - [6 - [（取代氨基）苯基] -1,2-二氢-2-氧代烟酰基] -2-取代的甘氨酸。还公开了含有所述化合物的药物组合物和使用所述组合物治疗感染的方法。

5. 发明授权

US3948903A Substituted N-(1,2-dihydro-2-oxonicotinyl)-cephalexins and -cephaloglycins 失效
标题翻译：取代的N-（1,2-二氢-2-氧代烟酰基） - 脑啡肽和脑胶质
公开(公告)号：US3948903A
公开(公告)日：1976-04-06
申请号：US522569
申请日：1974-11-11
申请人： Leonard Doub , James S. Kaltenbronn
发明人： Leonard Doub , James S. Kaltenbronn
IPC分类号： C07D213/80 , C07D213/85 , C07D221/16 , C07D499/00 , C07D501/20 , C07D501/34
CPC分类号： C07D213/80 , C07D213/85 , C07D221/16 , C07D499/00
摘要： Novel organic amide compounds which are substituted N-(1,2-dihydro-2-oxonicotinyl)-ampicillins, -cephalexins and -cephaloglycins having broad spectrum antibacterial utility are provided by (a) reacting the free amino acid ampicillin, cephalexin or cephaloglycin or the acid salt or silylated derivative thereof with a reactive derivative of the corresponding 1,2-dihydro-2-oxonicotinic acid or (b) reacting the free amino acid 6-aminopenicillanic acid, 7-aminocephalosporanic acid or 7-amino-3-methylceph-3-em-4-carboxylic acid or the acid salt or silylated derivative thereof with a reactive derivative of the corresponding N-(1,2-dihydro-2-oxonicotinyl)-2-phenylglycine.
摘要翻译：通过（a）使游离氨基酸氨苄青霉素，头孢氨苄或头孢氨呋喃或者头孢氨苄或其他化合物反应，得到具有广谱抗菌效用的取代的N-（1,2-二氢-2-氧代烟碱基） - 滑环蛋白， - 脑啡肽和 - 其酸性盐或甲硅烷基化衍生物与相应的1,2-二氢-2-氧代烟酸的反应性衍生物或（b）使游离氨基酸6-氨基青霉烷酸，7-氨基头孢烷酸或7-氨基-3-甲基头孢 -3-em-4-羧酸或其酸式盐或甲硅烷基化衍生物与相应的N-（1,2-二氢-2-氧代烟酰基）-2-苯基甘氨酸的反应性衍生物。

6. 发明授权

US5260278A Diol-containing renin inhibitors 失效
标题翻译：含二醇的肾素抑制剂
公开(公告)号：US5260278A
公开(公告)日：1993-11-09
申请号：US678469
申请日：1991-04-01
申请人： Richard Himmelsbach , John C. Hodges , James S. Kaltenbronn , William C. Patt , Joseph T. Repine , Ila Sircar
发明人： Richard Himmelsbach , John C. Hodges , James S. Kaltenbronn , William C. Patt , Joseph T. Repine , Ila Sircar
IPC分类号： A61K38/00 , C07D233/54 , C07K5/065 , A61K37/02 , C07D265/30 , C07D295/26 , C07K5/06
CPC分类号： C07D233/64 , C07K5/06078 , A61K38/00 , Y10S530/86
摘要： The invention concerns novel renin-inhibitory peptides which are useful for treating renin-associated hypertension, congestive heart failure, hyperaldosteronism, and diseases caused by retroviruses including HTLV-I and -III. Processes for preparing the peptides, compositions containing them, and methods of using them are included. Also included is a diagnostic method which uses the compounds to determine the presence of renin-associated hypertension, or hyperaldosteronism.
摘要翻译：本发明涉及可用于治疗肾素相关性高血压，充血性心力衰竭，醛固酮增多症和由逆转录病毒（包括HTLV-1和-III）引起的疾病的新型肾素抑制肽。包括肽的制备方法，含有它们的组合物和使用它们的方法。还包括使用该化合物来确定肾素相关性高血压或醛固酮增多症的存在的诊断方法。

7. 发明授权

US4743585A Renin inhibitors 失效
标题翻译：肾素抑制剂
公开(公告)号：US4743585A
公开(公告)日：1988-05-10
申请号：US920330
申请日：1986-11-21
申请人： James P. Hudspeth , James S. Kaltenbronn , Elizabeth A. Lunney , Joseph T. Repine , W. Howard Roark , Michael A. Stier , Francis J. Tinney , Peter W. K. Woo , Ernest D. Nicolaides
发明人： James P. Hudspeth , James S. Kaltenbronn , Elizabeth A. Lunney , Joseph T. Repine , W. Howard Roark , Michael A. Stier , Francis J. Tinney , Peter W. K. Woo , Ernest D. Nicolaides
IPC分类号： C07K5/02 , A61K37/02 , C07K5/08 , C07K5/10 , C07K7/06
CPC分类号： C07K5/0227 , C07K5/0205 , C07K5/0207 , Y10S530/86 , Y10S930/27
摘要： The invention concerns novel renin-inhibitory peptides which are useful for treating renin associated hypertension and for treating hyperaldosteronism. Novel intermediates, processes for preparing both the intermediates and the novel peptides, pharmaceutical compositions, and methods of treatment are included.
摘要翻译：本发明涉及可用于治疗肾素相关性高血压和治疗醛固酮增多症的新型肾素抑制肽。包括新的中间体，制备中间体和新型肽的方法，药物组合物和治疗方法。

8. 发明授权

US4596819A Modified tripeptides 失效
标题翻译：修饰三肽
公开(公告)号：US4596819A
公开(公告)日：1986-06-24
申请号：US573233
申请日：1984-01-23
申请人： Ernest D. Nicolaides , Francis J. Tinney , James S. Kaltenbronn , Dana E. DeJohn , Elizabeth A. Lunney , W. Howard Roark , Joseph T. Repine
发明人： Ernest D. Nicolaides , Francis J. Tinney , James S. Kaltenbronn , Dana E. DeJohn , Elizabeth A. Lunney , W. Howard Roark , Joseph T. Repine
IPC分类号： C07D203/20 , C07D207/08 , C07D207/09 , C07D207/16 , C07D207/26 , C07D207/277 , C07D207/28 , C07D207/48 , C07D213/81 , C07D241/08 , C07D265/32 , C07D333/38 , C07D403/12 , C07D498/04 , C07K5/06 , C07K5/068 , A61K31/34 , C07D207/12
CPC分类号： C07D207/08 , C07D203/20 , C07D207/09 , C07D207/16 , C07D207/277 , C07D207/28 , C07D207/48 , C07D213/81 , C07D241/08 , C07D265/32 , C07D333/38 , C07D403/12 , C07K5/06043 , C07K5/06086 , Y10S930/15
摘要： Modified oxytocin-vasopressin di- or tri-peptides wherein an amide group is replaced by a group selected from ##STR1## --CH.sub.2 NH--, --CH.sub.2 O--, --CH.sub.2 S--, --CH.sub.2 SO--, --CH.sub.2 SO.sub.2 --, --CH.sub.2 CH.sub.2 -- and --CH.dbd.CH-- are described as well as methods for their manufacture, pharmaceutical compositions and methods for treatment, especially of cognitive disorders, depression, morphine dependency and parkinsonism by adjunctive therapy.
摘要翻译：改性催产素 - 加压素二或三肽，其中酰胺基被选自下组的基团替代：-CH 2 NH - ， - CH 2 O - ， - CH 2 S - ， - CH 2 SO - ， - CH 2 SO 2 - ， - CH 2 CH 2 - 和-CH 描述了它们的制备方法，药物组合物和治疗方法，特别是认知障碍，抑郁症，吗啡依赖性和帕金森综合征的辅助治疗方法。

9. 发明授权

US6008372A Substituted dinaphthylmethyl and diheteroarylmethylacetyl histidine inhibitors of protein farnesyltransferase 失效
标题翻译：蛋白质法呢基转移酶的取代二萘基甲基和二杂芳基甲基乙酰基组氨酸抑制剂
公开(公告)号：US6008372A
公开(公告)日：1999-12-28
申请号：US101206
申请日：1998-07-02
申请人： Annette M. Doherty , James S. Kaltenbronn , Daniele Leonard , John Quin, III , Jeffrey D. Scholten
发明人： Annette M. Doherty , James S. Kaltenbronn , Daniele Leonard , John Quin, III , Jeffrey D. Scholten
IPC分类号： C07D233/54 , C07D233/64 , C07D409/12 , C07D409/14 , A61K31/41 , A61K31/535 , C07D413/12
CPC分类号： C07D233/64 , C07D409/12 , C07D409/14
摘要： Substituted histidine compounds of formula (I) are described as well as methods for the preparation and pharamaceutical compositions of same, which are useful as inhibitors of protein famesyltransferase and for the treatment of proliferative diseases including cancer, restenosis, and psoriasis, and as antiviral agents. ##STR1##
摘要翻译： PCT No.PCT / US97 / 00265 Sec。 371日期：1998年7月2日 102（e）日期1998年7月2日PCT 1997年1月2日PCT公布。公开号WO97 / 26246 日期1997年7月24日描述了式（I）的取代的组氨酸化合物以及其制备方法和相同的药物组合物，其可用作蛋白质法呢基转移酶的抑制剂和用于治疗增殖性疾病，包括癌症，再狭窄和牛皮癣，以及作为抗病毒剂。

10. 发明授权

US5610177A Acylated amino acids as endothelin antagonists 失效
标题翻译：酰基化氨基酸作为内皮素拮抗剂
公开(公告)号：US5610177A
公开(公告)日：1997-03-11
申请号：US287389
申请日：1994-08-08
申请人： Annette M. Doherty , Harriet W. Hamilton , James S. Kaltenbronn , John Quin, III
发明人： Annette M. Doherty , Harriet W. Hamilton , James S. Kaltenbronn , John Quin, III
IPC分类号： C07D209/20 , C07D405/14 , A61K31/495 , A61K31/535 , C07D401/06 , C07D403/06 , C07D413/06 , A61K3/405 , A61K3/445
CPC分类号： C07D405/14 , C07D209/20
摘要： Novel acylated amino acids which are antagonists of endothelin are described. Methods for their preparation and pharmaceutical compositions containing them are also included. The compounds are expected to be useful in treating elevated levels of endothelin, acute and chronic renal failure, hypertension, myocardial infarction, myocardial ischemia, cerebral vasospasm, cirrhosis, septic shock, congestive heart failure, endotoxic shock, subarachnoid hemorrhage, arrhythmias, asthma, preeclampsia, atherosclerotic disorders including Raynaud's disease and restenosis, angina, cancer, pulmonary hypertension, ischemic disease, gastric mucosal damage, hemorrhagic shock, ischemic bowel disease, diabetes, head injury, and stroke.
摘要翻译：描述了作为内皮素拮抗剂的新型酰化氨基酸。还包括其制备方法和含有它们的药物组合物。预期这些化合物可用于治疗高水平的内皮素，急性和慢性肾衰竭，高血压，心肌梗塞，心肌缺血，脑血管痉挛，肝硬化，脓毒性休克，充血性心力衰竭，内毒素性休克，蛛网膜下腔出血，心律失常，哮喘，先兆子痫，动脉粥样硬化疾病包括雷诺氏病和再狭窄，心绞痛，癌症，肺动脉高压，缺血性疾病，胃粘膜损伤，出血性休克，缺血性肠病，糖尿病，头部损伤和中风。

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