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1. 发明申请

WO1992016214A1 THE USE OF 5-AMINOSALICYLIC ACID IN THE TREATMENT OF IRRITABLE BOWEL SYNDROME - DIARRHEAL PHASE OR TYPE (IBS-D) 审中-公开
标题翻译： 5-氨基乙酸用于治疗可疑牙刷综合征 - 肾上腺皮质类型（IBS-D）
公开(公告)号：WO1992016214A1
公开(公告)日：1992-10-01
申请号：PCT/US1992000815
申请日：1992-01-31
申请人： NORWICH EATON PHARMACEUTICALS INC.
发明人： NORWICH EATON PHARMACEUTICALS INC. , CLOYD, George, Gilbert , FELARCA, Allison, Barretto
IPC分类号： A61K31/60
CPC分类号： A61K31/60 , A61K9/0031 , A61K9/2081 , A61K9/2846 , A61K9/5073
摘要： Treatment for a human or other mammal afflicted with IBS-D, comprising the topical delivery to the intestinal tract of said human or other mammal, preferably the large intestine, of a safe and effective amount of a pharmaceutical composition consisting essentially of the 5-ASA active ingredient and pharmaceutically acceptable excipients. Said topical delivery is preferably accomplished by the oral administration to said human or other mammal of a delayed-release composition consisting essentially of said 5-ASA active ingredient and a pharmaceutically acceptable excipient.
摘要翻译：治疗患有IBS-D的人或其他哺乳动物，其包括将所述人或其它哺乳动物（优选大肠）的肠道局部递送至安全有效量的基本上由5-ASA组成的药物组合物活性成分和药学上可接受的赋形剂。所述局部递送优选通过向所述人或其他哺乳动物口服施用基本上由所述5-ASA活性成分和药学上可接受的赋形剂组成的延迟释放组合物来完成。

2. 发明申请

WO1990004595A1 NOVEL ANTIMICROBIAL FLUOROQUINOLONYL CEPHEMS 审中-公开
标题翻译：新型抗微生物氟代喹啉CEPHEMS
公开(公告)号：WO1990004595A1
公开(公告)日：1990-05-03
申请号：PCT/US1989004768
申请日：1989-10-24
申请人： NORWICH EATON PHARMACEUTICALS, INC.
发明人： NORWICH EATON PHARMACEUTICALS, INC. , DEMUTH, Thomas, Prosser, Jr. , WHITE, Ronald, Eugene
IPC分类号： C07D501/48
CPC分类号： C07D501/34 , C07D501/26
摘要： Antimicrobial fluoroquinolonyl cephems of formula (I), wherein (1) R?1 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 unsubstitued piperazine, 3-aminopyrrolidine, or 3-aminomethylpyrrolidine. R4 is preferably hydrogen or halogen.

3. 发明申请

WO1990004591A1 NOVEL ANTIMICROBIAL DITHIOCARBAMOYL QUINOLONES 审中-公开
标题翻译：新型抗微生物二硫代喹啉喹诺酮
公开(公告)号：WO1990004591A1
公开(公告)日：1990-05-03
申请号：PCT/US1989004806
申请日：1989-10-24
申请人： NORWICH EATON PHARMACEUTICALS, INC.
发明人： NORWICH EATON PHARMACEUTICALS, INC. , DEMUTH, Thomas, Prosser, Jr. , WHITE, Ronald, Eugene
IPC分类号： C07D401/04
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 general formula (I), wherein A?1, 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 R1 is X, R3 is X, or both R?1 and R3¿ are X; and X is -R?15-N(R16)(R17) or -R15-R18-N(R19)(R17¿), where R15 is nil, alkyl, a carbocyclic ring, or a heterocyclic ring; and R16 is hydrogen, alkyl, alkenyl, a carbocyclic ring, a heterocyclic ring; or when X is R?15-N(R16)(R17), R16 and R15¿ may together comprise a heterocyclic ring including the nitrogen atom to which R?15 and R16¿ are bonded; R17 is C(=S)-S-M, where M is a pharmaceutically acceptable salt or biohydrolyzable ester; and R18 is alkyl, a carbocyclic ring, or a heterocyclic ring; and R19 is hydrogen, alkyl, alkenyl, a carbocyclic ring, a heterocyclic ring; or R?18 and R19¿ may together comprise a heterocyclic ring including the nitrogen atom to which R?18 and R19¿ are bonded; and pharmaceutically-acceptable salts and biohydrolyzable esters thereof, and hydrates thereof.

4. 发明申请

WO1992016206A1 THE USE OF 5-AMINOSALICYLIC ACID IN THE TREATMENT OF IRRITABLE BOWEL SYNDROME - DIARRHEAL PHASE OR TYPE (IBS-D) 审中-公开
标题翻译： 5-氨基乙酸用于治疗可疑牙刷综合征 - 肾上腺皮质类型（IBS-D）
公开(公告)号：WO1992016206A1
公开(公告)日：1992-10-01
申请号：PCT/US1992001848
申请日：1992-03-05
申请人： NORWICH EATON PHARMACEUTICALS INC.
发明人： NORWICH EATON PHARMACEUTICALS INC. , CLOYD, George, Gilbert , FELARCA, Allison, Barretto
IPC分类号： A61K31/40
CPC分类号： A61K31/60 , A61K9/0031 , A61K9/2081 , A61K9/2846 , A61K9/5073
摘要： Treatment for a human or other mammal afflicted with IBS-D, comprising the topical delivery to the intestinal tract of said human or other mammal, preferably the large intestine, of a safe and effective amount of a pharmaceutical composition consisting essentially of the 5-ASA active ingredient and pharmaceutically-acceptable excipients. Said topical delivery is preferably accomplished by the oral administration to said human or other mammal of a delayed-release composition consisting essentially of said 5-ASA active ingredient and a pharmaceutically-acceptable excipient.
摘要翻译：治疗患有IBS-D的人或其他哺乳动物，其包括将所述人或其它哺乳动物（优选大肠）的肠道局部递送至安全有效量的基本上由5-ASA组成的药物组合物活性成分和药学上可接受的赋形剂。所述局部递送优选通过向所述人或其他哺乳动物口服施用基本上由所述5-ASA活性成分和药学上可接受的赋形剂组成的延迟释放组合物来完成。

5. 发明申请

WO1991016327A1 ANTIMICROBIAL QUINOLONYL LACTAMS 审中-公开
标题翻译：抗微生物喹诺酮类LACTAMS
公开(公告)号：WO1991016327A1
公开(公告)日：1991-10-31
申请号：PCT/US1991002476
申请日：1991-04-12
申请人： NORWICH EATON PHARMACEUTICALS, INC.
发明人： NORWICH EATON PHARMACEUTICALS, INC. , DEMUTH, Thomas, Prosser, Jr. , WHITE, Ronald, Eugene
IPC分类号： C07D501/28
CPC分类号： C07D477/14 , C07D477/20 , C07D499/00 , C07D499/88 , C07D501/00
摘要： Antimicrobial quinolonyl lactam compounds comprising a lactam-containing moiety linked to a quinolone moiety, of formula (I), wherein (1) A , A , A , R , and R generally form any of a variety of quinolone, naphthyridine or related cyclic moieties known in the art to have antimicrobial activity; and (2) R is part of a linking moiety, linking hte quinolone moiety to a lactam-containing moiety having formula (II), wherein (3) R , R , R , R , and R , together with bonds ''a'' and ''b'', form any of a variety of lactam-containing moieties known in the art to have antimicrobial activity; and (4) the linking moiety includes (for example) carbamate, dithiocarbamate, urea, thiourea, isouronium, isothiouronium, guanidine, carbonate, trithiocarbonate, reversed carbamate, xanthate, reversed isouronium, reversed dithiocarbamate, reversed isothiouronium, amine, imine, ammonium, heteroarylium, ether, thioether, ester, thioester, amide, and hydrazide groups.
摘要翻译：包含与式（I）的喹诺酮部分连接的含内酰胺部分的抗微生物喹诺酮内酰胺化合物，其中（1）A 1，A 2，A 3，R 1和R 4 >通常形成本领域已知的各种喹诺酮，萘啶或相关的环状部分以具有抗微生物活性; 和（2）R 6是连接部分的一部分，将喹诺酮部分与具有式（II）的含内酰胺部分连接，其中（3）R 10，R 11，R 12， R 13和R 14与键“a”和“b”一起形成本领域已知的具有抗微生物活性的各种含内酰胺的部分; 连接部分包括（例如）氨基甲酸酯，二硫代氨基甲酸酯，脲，硫脲，异脲，异硫脲，胍，碳酸酯，三硫代碳酸酯，反相氨基甲酸酯，黄原酸酯，反式异卤素，反式二硫代氨基甲酸酯，反式异硫脲，胺，亚胺，杂芳基，醚，硫醚，酯，硫酯，酰胺和酰肼基团。

6. 发明申请

WO1992014474A1 METHODS FOR THE TREATMENT OF OSTEOPOROSIS 审中-公开
标题翻译：治疗骨质疏松症的方法
公开(公告)号：WO1992014474A1
公开(公告)日：1992-09-03
申请号：PCT/US1992000854
申请日：1992-01-31
申请人： NORWICH EATON PHARMACEUTICALS, INC.
发明人： NORWICH EATON PHARMACEUTICALS, INC. , McOSKER, Jocelyn, Elaine
IPC分类号： A61K31/66
CPC分类号： A61K31/66 , A61K31/565 , A61K2300/00
摘要： Methods of treatment for osteoporosis in a human or other animal subject, comprising: administering a bone-active phosphonate to said subject, at a level of at least about 0.1 LED per day of said treatment; and administering an estrogen hormone to said subject at a level of from about 0.2 to about 0.8 LED per day of said treatment. The bone-active phosphonate is preferably a bisphosphonate, or a phosphonoalkyl phosphonate.
摘要翻译：治疗人或其他动物受试者的骨质疏松症的方法，包括：以所述治疗的每天至少约0.1LL的水平向所述受试者施用骨 - 活性膦酸盐; 并且以所述治疗的每天约0.2至约0.8L LED的水平向所述受试者施用雌激素。骨活性膦酸盐优选为双膦酸盐或膦酰基烷基膦酸盐。

7. 发明申请

WO1991016310A1 ANTIMICROBIAL QUINOLONE THIOUREAS 审中-公开
标题翻译：抗微生物喹诺酮类药物
公开(公告)号：WO1991016310A1
公开(公告)日：1991-10-31
申请号：PCT/US1991002203
申请日：1991-04-01
申请人： NORWICH-EATON PHARMACEUTICALS, INC.
发明人： NORWICH-EATON PHARMACEUTICALS, INC. , DEMUTH, Thomas, Prosser, Jr. , WHITE, Ronald, Eugene
IPC分类号： C07D215/00
CPC分类号： C07D401/04 , C07D215/56 , C07D401/12 , C07D401/14 , C07D417/14 , C07D455/04 , C07D471/04 , C07D477/10 , C07D487/04 , C07D499/00 , C07D501/00 , C07D503/00 , C07D505/00 , C07D513/04
摘要： Antimicrobial quinolone thiourea compounds of general formula (I), wherein (1) A , A , A , R , R , R , and R 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) R is X, R is X, or both R and R are X; and (2) X is -R -N(R )(R ) or -R -R -N(R )(R ), where (a) (1) R is nil, alkyl, a carbocyclic ring, or a heterocyclic ring; and (2) R is hydrogen; alkyl; alkenyl; a carbocyclic ring; a heterocyclic ring; or (3) when X is R -N(R )(R ), R and R may together comprise a heterocyclic ring including the nitrogen atom to which R and R are bonded; (b) R is C(=S)-NR R ; where R is hydrogen, alkyl, alkenyl, a carbocyclic ring or a heterocyclic ring; and R is R or N(R )(R ); or R and R , together with the nitrogen to which they are bonded, form a heterocyclic ring; and (c) (1) R ) is alkyl, a carbocyclic ring, or a heterocyclic ring; and (2) R is hydrogen; alkyl; alkenyl; a carbocyclic ring; a heterocyclic ring; or (3) R and R may together comprise a heterocyclic ring including the nitrogen atom to which R and R are bonded; and pharmaceutically-acceptable salts and biohydrolyzable esters thereof, and hydrates thereof.
摘要翻译：通式（I）的抗菌喹诺酮硫脲化合物，其中（1）A 1，A 2，A 3，R 1，R 3，R 4和R 6，形成与本领域已知的具有抗微生物活性的各种喹诺酮和相关杂环结构中的任何一种; 和（2）（1）R 1是X，R 3是X，或者R 1和R 3都是X; 和（2）X是-R 15 -N（R 16）（R 17）或-R 15 -R 18 -N（R 19）（R 17）其中（a）（1）R 15为无，烷基，碳环或杂环; 和（2）R 16是氢; 烷基; 烯基; 碳环杂环; 或（3）当X是R 15 -N（R 16）（R 17）时，R 16和R 15可以一起包含包含氮原子的杂环，R 15 >和R 16键合; （b）R 17是C（= S）-NR 20 R 21; 其中R 20为氢，烷基，烯基，碳环或杂环; 并且R 21是R 20或N（R 20）（R 20）; 或R 20和R 21与它们所键合的氮一起形成杂环; 和（c）（1）R 18）是烷基，碳环或杂环; 和（2）R 19是氢; 烷基; 烯基; 碳环杂环; 或（3）R 18和R 19可以一起包含包含R 18和R 19键合的氮原子的杂环; 及其药学上可接受的盐和可生物水解的酯，及其水合物。

8. 发明申请

WO1990004594A1 NOVEL ANTIMICROBIAL QUINOLONYL LACTAM ESTERS 审中-公开
标题翻译：新型抗微生物喹诺酮乳酸酯
公开(公告)号：WO1990004594A1
公开(公告)日：1990-05-03
申请号：PCT/US1989004803
申请日：1989-10-24
申请人： NORWICH EATON PHARMACEUTICALS, INC.
发明人： NORWICH EATON PHARMACEUTICALS, INC. , DEMUTH, Thomas, Prosser, Jr. , WHITE, Ronald, Eugene
IPC分类号： C07D489/00
CPC分类号： C07D401/12 , C07D417/14 , C07D463/18 , C07D477/10 , C07D487/04 , C07D499/00 , C07D505/00 , C07D513/04
摘要： Antimicrobial quinolonyl lactam esters comprising a lactam-containing moiety linked, by an ester group, to the 3-carboxy group of a quinolone moiety. These compounds are of formula (I), wherein (1) R?3, R4, and R5¿, together with bonds ''a'' and ''b'', form certain lactam-containing moieties similar to those known in the art to have antimicrobial activity; and (2) A, R?6, R7, and R8¿ form any of a variety of quinolone or napthyridine structures similar to those known in the art to have antimicrobial activity.

9. 发明公开

EP0404233A3 Novel use of 5-phenyl-2-furan esters, amides and ketones as neuroprotective agents 失效
标题翻译：作为神经保护剂的5-苯基-2-呋喃酯，氨基酸和酮类的新用途
公开(公告)号：EP0404233A3
公开(公告)日：1992-01-08
申请号：EP90201540.3
申请日：1990-06-14
申请人： Norwich Eaton Pharmaceuticals, Inc.
发明人： Drust, Eugene George
IPC分类号： A61K31/34 , A61K31/495
CPC分类号： A61K31/495 , A61K31/34
摘要： The present invention encompasses methods of using 5-phenyl-2-furan esters, amides and ketones and compositions thereof to prevent or limit neuronal death or degeneration in a human or lower animal. These methods comprise systemically administering to such human or other animal a safe and effective amount of a compound of the formula:
wherein
(1) X is halo or nil; and Y is a substituent selected from the group consisting of unsubstituted or halogen-substituted methyl, halo, nitro, amino, and methoxy; and (2) R is R¹C(O)OH, R¹C(O)N(R³)₂, N(R³)₂, OR¹N(R³)₂, R¹N(R³)₂, N(R²)R¹N(R³)₂, or N(R²)N(R³)₂; where
R¹ is C₁-C₃ alkyl which is unsubstituted or substituted with C₁-C₂ alkyl;
R² is hydrogen or lower alkyl; and
each R³ is, independently, hydrogen or lower alkyl; or both R³ groups are connected to form a saturated 5- or 6-membered heterocycle containing 1 or 2 heteroatoms selected from oxygen and nitrogen, and said heterocycle is unsubstituted or substituted with lower alkyl or hydroxy-substituted lower alkyl; or a pharmaceutically acceptable salt thereof.

10. 发明公开

EP0384514A3 Dual-action tablet 失效
标题翻译：双作用片
公开(公告)号：EP0384514A3
公开(公告)日：1991-04-03
申请号：EP90200313.6
申请日：1990-02-12
申请人： Norwich Eaton Pharmaceuticals, Inc.
发明人： Dansereau, Richard John , Kane, Michael John
IPC分类号： A61K9/24
CPC分类号： A61K9/209
摘要： The present invention provides a dual-action tablet composition comprising:
(a) an outer tablet comprising a first dose of active ingredient dispersed in a pH independent hydrophilic polymer matrix; and (b) an inner tablet comprising a second dose of active ingredient in a rapidly disintegrating excipient base. This dual-action tablet is especially efficacious for those active ingredients which half lives of less than two hours and which experience decreased absorption efficiency in the lower gastrointestinal tract. Among the preferred dual-action tablet composition is one wherein the active ingredient in both the inner and outer tablets is guaifenesin. Upon administration, the outer tablet provides a controlled release of the active ingredient while the inner tablet gives a second dose of active ingredient after the outer tablet has partially dissolved.

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