公开(公告)号：EP0230068B1

公开(公告)日：1992-07-15

申请号：EP86202168.0

申请日：1986-12-04

申请人： Norwich Eaton Pharmaceuticals, Inc.

发明人： Benedict, James John ,  Perkins, Christopher Mark

IPC分类号： A61K31/675 ,  C07F9/58 ,  C07F9/547

CPC分类号： C07F9/65122 ,  C07F9/582

公开(公告)号：EP0366193A3

公开(公告)日：1992-01-08

申请号：EP89202646.9

申请日：1989-10-19

申请人： Norwich Eaton Pharmaceuticals, Inc.

发明人： Demuth, Thomas Prosser, Jr. ,  White, Ronald Eugene

IPC分类号： C07D499/88 ,  C07D519/00 ,  C07D487/04 ,  C07D401/12 ,  C07D471/04 ,  C07D501/20 ,  C07D513/04 ,  C07D417/14 ,  C07D498/047 ,  C07D401/14 ,  C07D499/84

CPC分类号： C07D401/12 ,  C07D401/14 ,  C07D417/14 ,  C07D463/12 ,  C07D463/20 ,  C07D463/22 ,  C07D471/04 ,  C07D477/10 ,  C07D487/04 ,  C07D499/00 ,  C07D503/00 ,  C07D505/00 ,  C07D513/04

摘要： Antimicrobial quinolonyl lactam compounds comprising a lactam-containing moiety linked, by a non-ester linking moiety, to the 3-carboxy group of a quinolone moiety. These compounds are of the formula:
wherein
(1) R 3 , R 4 , and R 5 , together with bonds "a" and "b", form any of a variety of lactam-containing moieties similar to those known in the art to have antimicrobial activity; (2) A, R 6 , R 7 , and R 8 form any of a variety of quinolone or naphthyridine structures similar to those known in the art to have antimicrobial activity; and (3) Y, together with R 5 , form a variety of non-ester linking moieties between the lactam-containing moiety and the quinolone moiety.

公开(公告)号：EP0366643A3

公开(公告)日：1991-12-04

申请号：EP89870161.0

申请日：1989-10-24

申请人： Norwich Eaton Pharmaceuticals, Inc.

发明人： Demuth, Thomas Prosser, Jr. ,  White, Ronald Eugene

IPC分类号： C07D215/56 ,  C07D471/04 ,  C07D498/06 ,  C07D513/04 ,  C07D519/00 ,  C07D487/08 ,  C07D401/04 ,  C07D498/04 ,  C07D471/06 ,  C07D513/06 ,  C07D413/04

CPC分类号： C07D401/04 ,  C07D215/56 ,  C07D401/12 ,  C07D401/14 ,  C07D417/14 ,  C07D455/04 ,  C07D471/04 ,  C07D477/10 ,  C07D487/04 ,  C07D499/00 ,  C07D503/00 ,  C07D505/00 ,  C07D513/04

摘要： Antimicrobial dithiocarbamoyl quinolone compounds of the general formula:
wherein
(1) A¹, A², A³, R¹, R³, R⁴, and R⁶ form any of a variety of quinolone and related heterocyclic structures similar to those known in the art to have antimicrobial activity; and (2)
(1) R¹ is X, R³ is X, or both R¹ and R³ are X; and (2) X is -R¹⁵-N(R¹⁶)(R¹⁷) or -R¹⁵-R¹⁸-N(R¹⁹)(R¹⁷), where (a) (1) R¹⁵ is nil, alkyl, a carbocyclic ring, or a heterocyclic ring; and
(2) R¹⁶ is hydrogen; alkyl; alkenyl; a carbocyclic ring; a heterocyclic ring; or
(3) when X is R¹⁵-N(R¹⁶)(R¹⁷), R¹⁶ and R¹⁵ may together comprise a heterocyclic ring including the nitrogen atom to which R¹⁵ and R¹⁶ are bonded; (b) R¹⁷ is C(=S)-S-M, where M is a pharmaceutically-­acceptable salt or biohydrolyzable ester; and
(c) (1) R¹⁸ is alkyl, a carbocyclic ring, or a heterocyclic ring; and
(2) R¹⁹ is hydrogen; alkyl; alkenyl; a carbocyclic ring; a heterocyclic ring; or
(3) R¹⁸ and R¹⁹ may together comprise a heterocyclic ring including the nitrogen atom to which R¹⁸ and R¹⁹ are bonded; and pharmaceutically-acceptable salts and biohydrolyzable esters thereof, and hydrates thereof.

公开(公告)号：EP0366640A2

公开(公告)日：1990-05-02

申请号：EP89870151.1

申请日：1989-10-20

申请人： Norwich-Eaton Pharmaceuticals, Inc.

发明人： Demuth, Thomas Prosser, Jr. ,  White, Ronald Eugene

IPC分类号： C07D501/26 ,  A61K31/545

CPC分类号： C07D501/34 ,  C07D501/26

摘要： Antimicrobial fluoroquinolonyl cephems of the formula:
wherein

(1) R¹ and R² are groups among those known in the art for substitution at the 7-position of an antimicrobially-active cephem;
(2) R³ is a substituted or unsubstituted, nitrogen-containing, heterocyclic moiety; and
(3) R⁴ is hydrogen, halogen, lower alkoxy or cyclic alkoxy, amino, nitro or cyano.

Preferably, R³ is substituted or unsubstituted piperazine, 3-aminopyrrolidine, or 3-aminomethylpyrrolidine. R⁴ is preferably hydrogen or halogen.

摘要翻译： 其中（1）R 1和R 2是本领域已知的用于在抗微生物活性头孢烯的7位置换的基团，其具有下式的抗微生物氟喹诺酮基头孢烯： （2）R 3是取代或未取代的含氮杂环部分; 和（3）R 4是氢，卤素，低级烷氧基或环烷氧基，氨基，硝基或氰基。 优选地，R 3是取代或未取代的哌嗪，3-氨基吡咯烷或3-氨基甲基吡咯烷。 R 4优选为氢或卤素。

公开(公告)号：EP0188107A3

公开(公告)日：1989-07-05

申请号：EP85309139.5

申请日：1985-12-16

申请人： Norwich Eaton Pharmaceuticals, Inc.

发明人： Burch, Homer Albert ,  Ebetino, Frank Frederick

IPC分类号： A61K31/535

CPC分类号： A61K31/535

摘要： The invention involves a method of treating malignant tumors in a mammal with the compound ethyl 4-hydroxy-2-[15-morpholinomethyl-2-oxo)-3-oxazolidiny- liminomethyl]furo[2,3-b[pyridine-5-carboxylate (Compound 1) or its pharmaceutically acceptable salts or hydrates.

公开(公告)号：EP0304987A2

公开(公告)日：1989-03-01

申请号：EP88201734.6

申请日：1988-08-15

申请人： Norwich Eaton Pharmaceuticals, Inc.

发明人： Jacobs, Stephen Allen

IPC分类号： A61K31/19 ,  A23L1/29

CPC分类号： A61K31/19 ,  C07C59/245 ,  C07C59/265

摘要： A calcium citrate malate complex or mixture having a molar composition of calcium:citrate:malate of about 6:2:3. The calcium citrate malate is preferably administered in an oral dosage form, containing pharmaceutically-acceptable carriers and excipients.

摘要翻译： 柠檬酸钙苹果酸盐复合物或具有约6:2:3的钙：柠檬酸盐：苹果酸盐的摩尔组成的混合物。 柠檬酸苹果酸钙优选以口服剂型施用，其含有药学上可接受的载体和赋形剂。

公开(公告)号：EP0304986A2

公开(公告)日：1989-03-01

申请号：EP88201733.8

申请日：1988-08-15

申请人： Norwich Eaton Pharmaceuticals, Inc.

发明人： Kochanowski, Barbara Ann

IPC分类号： A61K31/19 ,  A23L1/29 ,  A23L2/26

CPC分类号： A61K31/19 ,  A23L33/165

摘要： Methods for building bone in a human or other animal subject, comprising administering to said subject a safe and effective amount of calcium citrate malate. The calcium citrate malate is preferably administered for at least about three months. A preferred method of the invention is for the treatment of osteoporosis. The calcium citrate malate comprises a complex of a mixture of calcium salts having a ratio of moles citrate to moles malate of from about 1:0.16 to about 1:13.5. The calcium citrate malate is preferably administered in an oral dosage form, containing pharmaceutically-acceptable carriers and excipients.

摘要翻译： 方法用于在人或其他动物受试者构建骨，包括给予所述受试者柠檬酸苹果酸钙的安全和有效量。 柠檬酸苹果酸钙优选施用至少约3个月。 本发明的优选的方法是用于治疗骨质疏松症。 柠檬酸苹果酸钙包括具有摩尔柠檬酸盐以约1的摩尔苹果酸的比率钙盐的混合物的复合物：0:16至约1：5.13。 柠檬酸苹果酸钙，优选的剂量形式口服给药，含有药学上可接受的载体和赋形剂。

公开(公告)号：EP0271151A3

公开(公告)日：1988-07-27

申请号：EP87202383

申请日：1987-12-02

申请人： Norwich Eaton Pharmaceuticals, Inc.

发明人： Schwe, Fang Pong

IPC分类号： A61K31/42 ,  A61K09/32 ,  A61K09/52

CPC分类号： A61K9/5026 ,  A61K9/2846 ,  A61K31/42

摘要： The invention involves a method for achieving systemic adminis­tration of azumolene by delivering the drug to the intestines without exposing the drug in the stomach, and pharmaceutical compositions for achieving such administration of azumolene.

摘要翻译： 本发明涉及一种通过将药物递送至肠而不暴露胃中的药物来实现全身给药的方法，以及用于实现这种阿舒姆莱的给药的药物组合物。

公开(公告)号：EP0187705A3

公开(公告)日：1988-05-11

申请号：EP86300057

申请日：1986-01-07

申请人： Norwich Eaton Pharmaceuticals, Inc.

发明人： Alaimo, Robert James ,  Anderson, Jon Alan

IPC分类号： A61K31/47 ,  C07D471/04 ,  C07D405/04 ,  C07D307/68 ,  C07D235/08 ,  C07D235/06 ,  C07D235/00 ,  C07D221/00

CPC分类号： C07D235/06 ,  C07D235/08 ,  C07D307/68 ,  C07D405/04 ,  C07D471/04

摘要： The present invention involves compounds of the class of imidazo[4, 5-f]quinolines and methods for enhancing the immune response system of mammals which comprises systemically administering to mammals having a depressed immune function an effective but nontoxic amount of a composition comprising such a compound.

公开(公告)号：EP0187705A2

公开(公告)日：1986-07-16

申请号：EP86300057.6

申请日：1986-01-07

申请人： Norwich Eaton Pharmaceuticals, Inc.

发明人： Alaimo, Robert James ,  Anderson, Jon Alan

IPC分类号： A61K31/47 ,  C07D471/04

CPC分类号： C07D235/06 ,  C07D235/08 ,  C07D307/68 ,  C07D405/04 ,  C07D471/04

摘要： The present invention involves compounds of the class of imidazo[4, 5-f]quinolines and methods for enhancing the immune response system of mammals which comprises systemically administering to mammals having a depressed immune function an effective but nontoxic amount of a composition comprising such a compound.

摘要翻译： 本发明涉及咪唑并[4,5-f]喹啉类的化合物和用于增强哺乳动物的免疫应答系统的方法，该方法包括向具有抑制免疫功能的哺乳动物全身施用有效但无毒量的包含这种 复合。