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61. 发明授权

US5679675A 8-amino-10-(azabicycloalkyl)-pyrido�1,2,3-d,e!�1,3,4!benzoxadiazine derivatives 失效
标题翻译： 8-氨基-10-（氮杂双环烷基） - 吡啶并[1,2,3-d，e] [1,3,4]苯并恶二嗪衍生物
公开(公告)号：US5679675A
公开(公告)日：1997-10-21
申请号：US434806
申请日：1995-05-04
申请人： Thomas Jaetsch , Burkhard Mielke , Uwe Petersen , Thomas Schenke , Klaus-Dieter Bremm , Rainer Endermann , Karl-Georg Metzger , Martin Scheer , Michael Stegemann , Heinz-Georg Wetzstein
发明人： Thomas Jaetsch , Burkhard Mielke , Uwe Petersen , Thomas Schenke , Klaus-Dieter Bremm , Rainer Endermann , Karl-Georg Metzger , Martin Scheer , Michael Stegemann , Heinz-Georg Wetzstein
IPC分类号： A61K9/00 , A61K31/535 , A61K31/5395 , A61P31/04 , C07D498/06 , C07D519/00
CPC分类号： C07D498/06
摘要： The present invention relates to new 8-amino-10-(azabicycloalkyl)-pyrido�1,2,3-d,e!�1,3,4!benzoxadiazine derivatives of the general formula (I) ##STR1## in which the radicals R.sup.1 to R.sup.4, Z and X.sup.1 have the meaning given in the description, processes for their preparation and their use in antibacterial compositions.
摘要翻译：本发明涉及通式（I）的新的8-氨基-10-（氮杂双环烷基） - 吡啶并[1,2,3-d，e] [1,3,4]苯并恶嗪衍生物。其中基团R1至R4，Z和X1具有说明书中给出的含义，其制备方法及其在抗菌组合物中的应用。

62. 发明授权

US5646163A Quinolone 5-(N-heterosubstituted amino) antimicrobials 失效
标题翻译：喹诺酮5-（N-异取代氨基）抗微生物剂
公开(公告)号：US5646163A
公开(公告)日：1997-07-08
申请号：US235003
申请日：1994-04-28
申请人： Thomas Prosser Demuth, Jr. , Ronald Eugene White
发明人： Thomas Prosser Demuth, Jr. , Ronald Eugene White
IPC分类号： A61K31/47 , A61K31/4709 , A61K31/495 , A61K31/535 , A61K31/54 , A61P31/00 , A61P31/04 , C07D215/56 , C07D401/04 , C07D413/04 , C07D471/04 , C07D487/04 , C07D487/08 , C07D498/04 , C07D498/06 , C07D498/14 , C07D498/16 , C07D513/04 , C07D513/06 , C07D513/14 , C07D513/16 , C07D515/04 , C07D215/233 , C07D215/58
CPC分类号： C07D215/56 , C07D401/04 , C07D513/04
摘要： The invention relates to antimicrobial 5-(N-heterosubstituted amino) quinolone compounds having a structure according to Formula (I) or (II): ##STR1## wherein (1) R.sup.1, R.sup.2, R.sup.3, R.sup.9 and R.sup.10 form any of a variety of quinolone and related heterocyclic structures similar to those known in the art to have antimicrobial activity; and(2)(a) R.sup.4 and R.sup.5 are, independently, hydrogen; lower alkyl; cycloalkyl; heteroalkyl; or --C(.dbd.O)--X--R.sup.8, where X is a covalent bond, N, O, or S, and R.sup.8 is lower alkyl, lower alkenyl, arylalkyl, a carbocylic ring, or a heterocyclic ring; or(b) R.sup.4 and R.sup.5 together comprise a heterocyclic ring that includes the nitrogen to which they are bonded;and the pharmaceutically-acceptable salts, biohydrolyzable esters, biohydrolyzable amides, and solvates thereof. The invention also relates to compositions comprising these compounds, as well as methods for treating infectious disorders using the compounds and/or compositions of the present invention.
摘要翻译：本发明涉及具有式（I）或（II）结构的抗微生物剂5-（N-异取代氨基）喹诺酮化合物：其中（1）R1，R2，R3 R9和R10形成与本领域已知的具有抗微生物活性相似的各种喹诺酮和相关杂环结构; 和（2）（a）R4和R5独立地是氢; 低级烷基环烷基杂烷基; 或-C（= O）-X-R 8，其中X为共价键，N，O或S，且R 8为低级烷基，低级烯基，芳基烷基，碳环或杂环。或（b）R4和R5一起包含杂环，其包括它们所键合的氮; 和药学上可接受的盐，生物可水解的酯，生物可水解的酰胺和溶剂合物。本发明还涉及包含这些化合物的组合物，以及使用本发明的化合物和/或组合物治疗感染性疾病的方法。

63. 发明授权

US5589476A Imidazol-4-ylpiperidine derivatives, their preparation and their application in therapeutics 失效
标题翻译：咪唑-4-基哌啶衍生物，其制备及其在治疗中的应用
公开(公告)号：US5589476A
公开(公告)日：1996-12-31
申请号：US317661
申请日：1994-10-03
申请人： Samir Jegham , G erard Defosse , Thomas A. Purcell , Luc Even
发明人： Samir Jegham , G erard Defosse , Thomas A. Purcell , Luc Even
IPC分类号： C07D401/14 , A61K31/445 , A61K31/47 , A61K31/495 , A61K31/535 , A61K31/55 , A61P1/00 , C07D233/54 , C07D413/14 , C07D471/06 , C07D487/06 , C07D498/06 , C07D498/12 , A61K31/435 , C07D498/16
CPC分类号： C07D471/06 , C07D487/06
摘要： A compound of formula (I): ##STR1## in which R.sub.1 represents a hydrogen atom or a straight or branched (C.sub.1 -C.sub.4)alkyl group; andA represents a 5,6-dihydro-4H-imidazo[4,5,1-ij]quinol-2-yl group, a 4,5-dihydroimidazo[1,5,4-de][1,4]benzoxazin-2-yl group, a 4-methyl-4,5-dihydroimidazo[1,5,4-de][1,4]benzoxazin-2-yl group, a 4-phenyl-4,5-dihydroimidazo[1,5,4-de][1,4]benzoxazin-2-yl group, a 4-phenylmethyl-4,5-dihydroimidazo[1,5,4-de][1,4]benzoxazin-2-yl group, a 5-methyl-4,5-dihydroimidazo[1,5,4-de][1,4]benzoxazin-2-yl group, a 5,6-dihydro-4H-imidazo[1,5,4-de]quinoxalin-2-yl group, a 6-oxo-5,6-dihydro-4H-imidazo[4,5,1-ij]quinol-2-yl group, or a 5-methyl-4,5,6,7-tetrahydroimidazo[4,5,1-jk][1,4]benzodiazepin-2-yl group which may be unsubstituted or substituted in the 6-position by a phenylmethyl group;or an addition salt thereof with a pharmaceutically acceptable acid.
摘要翻译：式（I）的化合物：其中R 1表示氢原子或直链或支链（C 1 -C 4）烷基; A代表5,6-二氢-4H-咪唑并[4,5,1-ij]喹啉-2-基，4,5-二氢咪唑并[1,5,4-de] [1,4]苯并恶嗪 -2-基，4-甲基-4,5-二氢咪唑并[1,5,4-de] [1,4]苯并恶嗪-2-基，4-苯基-4,5-二氢咪唑并[ 5,4-de] [1,4]苯并恶嗪-2-基，4-苯基甲基-4,5-二氢咪唑并[1,5,4-de] [1,4]苯并恶嗪-2-基， 5-甲基-4,5-二氢咪唑并[1,5,4-de] [1,4]苯并恶嗪-2-基，5,6-二氢-4H-咪唑并[1,5,4-de]喹喔啉 -2-基，6-氧代-5,6-二氢-4H-咪唑并[4,5,1-ij]喹啉-2-基或5-甲基-4,5,6,7-四氢 - 四氢咪唑并[4,5,1-jk] [1,4]苯并二氮杂-2-基，其可以未取代或在6-位被苯甲基取代; 或其与药学上可接受的酸的加成盐。

64. 发明授权

US5563138A Benzoheterocyclic compounds 失效
标题翻译：苯并杂环化合物
公开(公告)号：US5563138A
公开(公告)日：1996-10-08
申请号：US179239
申请日：1988-04-08
申请人： Hiraki Ueda , Hisashi Miyamoto , Hiroshi Yamashita , Hitoshi Tone
发明人： Hiraki Ueda , Hisashi Miyamoto , Hiroshi Yamashita , Hitoshi Tone
IPC分类号： C07D215/56 , A61K31/47 , A61K31/495 , A61K31/535 , A61K31/5375 , A61K31/54 , A61K31/55 , A61P31/04 , C07C25/02 , C07C25/13 , C07C63/04 , C07C63/06 , C07C63/70 , C07C69/716 , C07C69/738 , C07C205/11 , C07C205/12 , C07C211/47 , C07C211/52 , C07C229/30 , C07C229/34 , C07C321/16 , C07C323/29 , C07D207/09 , C07D207/14 , C07D215/22 , C07D241/04 , C07D295/04 , C07D295/16 , C07D319/06 , C07D401/04 , C07D405/06 , C07D405/12 , C07D409/04 , C07D413/04 , C07D487/04 , C07D491/04 , C07D498/04 , C07D498/06 , C07F5/04
CPC分类号： C07D491/04 , C07D215/56 , C07D401/04 , C07D405/12 , C07D409/04 , C07D487/04
摘要： Novel 4-oxoquinoline-3-carboxylic acid compounds of the formula: ##STR1## wherein R.sup.1 is cyclopropyl which may have 1 to 3 substituents of alkyl and halogen; phenyl which may be substituted by 1 to 3 substituents of alkoxy, halogen and OH; alkyl which may be substituted by halogen, alkanoyloxy or OH; alkenyl; or thienyl, R.sup.2 is 5- to 9-membered saturated or unsaturated heterocyclic ring which may be sustituted, R.sup.3 is alkyl, R is H or alkyl, and X is halogen, and pharmaceutically acceptable salts thereof, said compounds having excellent antimicrobial activity and hence being useful as an antimicrobial agent, and a pharmaceutical composition containing said compound as an active ingredient.
摘要翻译：具有下式的新型4-氧代喹啉-3-羧酸化合物：其中R 1是可以具有1至3个烷基和卤素取代基的环丙基; 可被1至3个烷氧基，卤素和OH取代基取代的苯基; 可被卤素，烷酰氧基或OH取代的烷基; 烯基; 或噻吩基，R 2为可被取代的5-至9-元饱和或不饱和杂环，R 3为烷基，R为H或烷基，X为卤素及其药学上可接受的盐，所述化合物具有优异的抗微生物活性，因此可用作抗微生物剂，以及含有所述化合物作为活性成分的药物组合物。

65. 发明授权

US5556979A 7-isoindolinyl-naphthyridone derivatives, compositions and anti-bacterial use thereof 失效
标题翻译： 7-异吲哚啉基 - 萘啶酮衍生物，其组合物和抗细菌用途
公开(公告)号：US5556979A
公开(公告)日：1996-09-17
申请号：US119369
申请日：1993-09-10
申请人： Thomas Philipps , Stephan Bartel , Andreas Krebs , Uwe Petersen , Thomas Schenke , Klaus-Dieter Bremm , Rainer Endermann , Karl G. Metzger , Burkhard Mielke
发明人： Thomas Philipps , Stephan Bartel , Andreas Krebs , Uwe Petersen , Thomas Schenke , Klaus-Dieter Bremm , Rainer Endermann , Karl G. Metzger , Burkhard Mielke
IPC分类号： A61K31/435 , A61K31/4035 , A61K31/4375 , A61K31/47 , A61K31/4709 , A61K31/535 , A61K31/5383 , A61K31/54 , A61K31/55 , A61P31/04 , C07D209/44 , C07D215/56 , C07D401/04 , C07D405/04 , C07D405/06 , C07D405/14 , C07D471/04 , C07D471/06 , C07D491/18 , C07D491/20 , C07D495/04 , C07D498/06 , C07D498/08 , C07D513/04 , C07D513/06 , C07D513/16 , C07D519/00
CPC分类号： C07D401/04 , C07D209/44 , C07D471/04 , C07D513/06
摘要： The invention relates to novel quinolone derivatives and naphthyridone derivatives which are substituted in the 7-position by a partially hydrogenated isoindolinyl ring, to processes for their preparation and to antibacterial agents and feed additives containing them.
摘要翻译：本发明涉及通过部分氢化的异吲哚啉基环在7-位被取代的新型喹诺酮衍生物和萘啶酮衍生物，其制备方法以及含有它们的抗菌剂和饲料添加剂。

66. 发明授权

US5534485A (2-imidazolin-2-yl) fused heteropyridine compounds, intermediates for the preparation of and use of said compounds as herbicidal agents 失效
公开(公告)号：US5534485A
公开(公告)日：1996-07-09
申请号：US458939
申请日：1995-06-02
申请人： Barrington Cross , Marinus Los , Robert F. Doehner, Jr. , David W. Ladner , Jerry L. Johnson
发明人： Barrington Cross , Marinus Los , Robert F. Doehner, Jr. , David W. Ladner , Jerry L. Johnson
IPC分类号： A01N43/90 , C07D401/04 , C07D471/04 , C07D491/04 , C07D491/048 , C07D491/052 , C07D491/056 , C07D491/10 , C07D491/14 , C07D491/147 , C07D495/04 , C07D497/04 , C07D498/04 , C07D498/22 , C07D513/04 , C07D498/06 , C07D513/06
CPC分类号： A01N43/90 , C07D401/04 , C07D471/04 , C07D491/04 , C07D491/10 , C07D491/14 , C07D495/04 , C07D497/04 , C07D513/04
摘要： There are provided novel (2-imidazolin-2-yl) fused heteropyridine compounds, and intermediate compounds for the preparation thereof, and a method for controlling a wide variety of annual and perennial plant species therewith.

67. 发明授权

US5495020A Benzoheterocyclic compounds 失效
标题翻译：苯并杂环化合物
公开(公告)号：US5495020A
公开(公告)日：1996-02-27
申请号：US562034
申请日：1990-08-02
申请人： Hiraki Ueda , Hisashi Miyamoto , Hiroshi Yamashita , Hitoshi Tone
发明人： Hiraki Ueda , Hisashi Miyamoto , Hiroshi Yamashita , Hitoshi Tone
IPC分类号： C07D215/56 , A61K31/47 , A61K31/495 , A61K31/535 , A61K31/5375 , A61K31/54 , A61K31/55 , A61P31/04 , C07C25/02 , C07C25/13 , C07C63/04 , C07C63/06 , C07C63/70 , C07C69/716 , C07C69/738 , C07C205/11 , C07C205/12 , C07C211/47 , C07C211/52 , C07C229/30 , C07C229/34 , C07C321/16 , C07C323/29 , C07D207/09 , C07D207/14 , C07D215/22 , C07D241/04 , C07D295/04 , C07D295/16 , C07D319/06 , C07D401/04 , C07D405/06 , C07D405/12 , C07D409/04 , C07D413/04 , C07D487/04 , C07D491/04 , C07D498/04 , C07D498/06 , C07F5/04
CPC分类号： C07D491/04 , C07D215/56 , C07D401/04 , C07D405/12 , C07D409/04 , C07D487/04
摘要： Useful as intermediates for antimicrobacterial agents are compounds of the formulas ##STR1## wherein R.sup.1A is a cyclopropyl which may be substituted by 1 to 3 substituents selected from the group consisting of a C.sub.1 -C.sub.6 alkyl and a halogen atom; a phenyl which may be substituted by 1 to 3 substituents selected from the group consisting of a C.sub.1 -C.sub.6 alkoxy, a halogen atom and hydroxy on the phenyl group; a C.sub.1 -C.sub.6 alkyl which may be substituted by a halogen atom, a C.sub.1 -C.sub.6 alkanoyloxy or hydroxy; a C.sub.2 -C.sub.6 alkenyl; or thienyl,R.sup.3A is a C.sub.1 -C.sub.6 alkyl group, or a halogen atom,R.sup.4 is a C.sub.1 -C.sub.6 alkyl group,R.sup.14 is a hydrogen atom, a lower alkyl group, or a group of the formula ##STR2## R.sup.31 is hydrogen or a C.sub.1 -C.sub.6 alkyl group, and X and X.sup.4 are halogen atoms, and salts thereof.
摘要翻译：作为抗微生物剂的中间体有用的是下式的化合物：其中R 1A是可以被1-3个选自C1-C6烷基和卤素原子的取代基取代的环丙基; 可以被1-3个选自C1-C6烷氧基，卤素原子和苯基上的羟基的取代基取代的苯基; 可被卤素原子取代的C1-C6烷基，C1-C6烷酰氧基或羟基; C 2 -C 6烯基; 或噻吩基，R 3A为C1-C6烷基或卤素原子，R4为C1-C6烷基，R14为氢原子，低级烷基或式为R3的基团为氢或 C 1 -C 6烷基，X和X 4为卤素原子，及其盐。

68. 发明授权

US5464796A 7-isoindolinyl-quinolone-carboxylic acid derivatives 失效
标题翻译： 7-异吲哚啉基 - 喹诺酮 - 羧酸衍生物
公开(公告)号：US5464796A
公开(公告)日：1995-11-07
申请号：US896955
申请日：1992-06-11
申请人： Uwe Petersen , Andreas Krebs , Thomas Schenke , Franz Kunisch , Thomas Philipps , Klaus Grohe , Klaus-Dieter Bremm , Rainer Endermann , Karl-Georg Metzger , Ingo Haller , Hans-Joachim Zeiler
发明人： Uwe Petersen , Andreas Krebs , Thomas Schenke , Franz Kunisch , Thomas Philipps , Klaus Grohe , Klaus-Dieter Bremm , Rainer Endermann , Karl-Georg Metzger , Ingo Haller , Hans-Joachim Zeiler
IPC分类号： A61K31/435 , A61K31/4375 , A61K31/44 , A61K31/47 , A61K31/4709 , A61K31/535 , A61P31/00 , A61P31/04 , C07D209/44 , C07D215/56 , C07D401/04 , C07D405/14 , C07D471/04 , C07D471/06 , C07D498/04 , C07D498/06 , C07D513/06 , C07D215/38
CPC分类号： C07D215/56 , C07D209/44 , C07D401/04 , C07D471/04
摘要： The invention relates to new quinolone- and naphthyridonecarboxylic acid derivatives which are substituted in the 7-position by a partly hydrogenated isoindolinyl ring, processes for their preparation and antibacterial agents and feed additives containing these compounds.
摘要翻译：本发明涉及通过部分氢化的异吲哚啉环在7位上被取代的新的喹诺酮和萘啶酮羧酸衍生物，其制备方法以及含有这些化合物的抗菌剂和饲料添加剂。

69. 发明授权

US5416096A 7-(1-pyrrolidinyl)-3-quinolone carboxylic acid derivatives as antibacterial agents and feed additives 失效
标题翻译： 7-（1-吡咯烷基）-3-喹诺酮羧酸衍生物作为抗菌剂和饲料添加剂
公开(公告)号：US5416096A
公开(公告)日：1995-05-16
申请号：US737631
申请日：1991-07-30
申请人： Uwe Petersen , Thomas Schenke , Andreas Krebs , Klaus Grohe , Michael Schriewer , Ingo Haller , Karl G. Metzger , Rainer Endermann , Hans-Joachim Zeiler
发明人： Uwe Petersen , Thomas Schenke , Andreas Krebs , Klaus Grohe , Michael Schriewer , Ingo Haller , Karl G. Metzger , Rainer Endermann , Hans-Joachim Zeiler
IPC分类号： A23K20/195 , A61K31/435 , A61K31/47 , A61K31/535 , A61P31/04 , C07D207/14 , C07D215/56 , C07D401/04 , C07D403/04 , C07D407/14 , C07D413/04 , C07D471/04 , C07D487/04 , C07D498/04 , C07D498/06 , C07D513/04 , C07D513/06 , C07D519/00 , C07D401/10
CPC分类号： C07D215/56 , C07D207/14 , C07D401/04 , C07D407/14 , C07D471/04 , C07D487/04 , C07D513/04
摘要： 7-(1-Pyrrolidinyl)-3-quinolone- and -naphthyridonecarboxylic acid derivatives as antibacterial agents and feed additives, of the formula ##STR1## in which X.sup.1 is halogen,X.sup.2 is hydrogen, halogen, amino or other radical,R.sup.1 is alkyl, cycloalkyl, optionally substituted phenyl or other radical,R.sup.2 is hydrogen, alkyl or a dioxolylmethyl radical,R.sup.3 is ##STR2## and A is N, CH, C-halogen, or the like, or forms a bridge with R.sup.1,and addition products thereof.
摘要翻译： 7-（1-吡咯烷基）-3-喹诺酮和 - 萘啶酮羧酸衍生物作为抗菌剂和饲料添加剂，其中X1是卤素，X2是氢，卤素，氨基或其它基团，R1是烷基，环烷基，任选取代的苯基或其它基团，R 2为氢，烷基或二氧杂环戊基甲基，R 3为甲基，A为N，CH，C-卤素等，或与R 1形成桥，及其加成产物。

70. 发明授权

US5273975A Heterocyclic amines having central nervous system activity 失效
标题翻译：具有中枢神经系统活性的杂环胺
公开(公告)号：US5273975A
公开(公告)日：1993-12-28
申请号：US778204
申请日：1991-12-06
申请人： Malcolm W. Moon , Richard F. Heier , Jeanette K. Morris
发明人： Malcolm W. Moon , Richard F. Heier , Jeanette K. Morris
IPC分类号： C07D215/40 , C07D455/04 , C07D471/06 , C07D498/06 , C07D513/06 , A61K31/495 , A61K31/50 , C07D513/02
CPC分类号： C07D471/06 , C07D215/40 , C07D455/04 , C07D513/06
摘要： Tricyclic nitrogen containing compounds, having central nervous system activity of the following structural formula: ##STR1## and pharmaceutically acceptable salts thereof wherein R.sub.1, R.sub.2, and R.sub.3 are independently hydrogen, C.sub.1-6 alkyl, alkenyl, or alkynyl, C.sub.3-10 cycloalkyl, or R.sub.1 and R.sub.2 are joined to form a C.sub.3-7 cyclic amine which can contain additional heteroatoms; X is hydrogen, C.sub.1-6 alkyl halogen, hydroxy, alkoxy, cyano, carboxamide, carboxyl, or carboalkoxyl; A is SO.sub.2, N, CH, CH.sub.2, CHCH.sub.3, C.dbd.O, C.dbd.S, C-SCH.sub.3, C.dbd.NH, C-NH.sub.2, C-NHCH.sub.3, C--NHCOOCH.sub.3, or C--NHCN. B is CH.sub.2, CH, C.dbd.O, N, NH or N--CH.sub.3 ; n is 0 or 1; and D is CH, CH.sub.2, C.dbd.O, O, N, NH or N--CH.sub.3. These new compounds are suitable for treating schizophrenia, Parkinson's disease, anxiety, depression or as compounds for lowering blood pressure in animal or human hosts.
摘要翻译： PCT No.PCT / US90 / 02621 Sec。 371 1991年12月6日第 102（e）1990年12月6日授权PCT 1990年5月15日提交PCT。具有以下结构式的中枢神经系统活性的三环氮化合物：其中R1，R2和R3独立地为氢，C 1-6烷基，烯基或炔基，C 3-10环烷基或R 1和R 2连接形成可含有其它杂原子的C 3-7环胺; X是氢，C 1-6烷基卤素，羟基，烷氧基，氰基，羧酰胺，羧基或烷氧羰基; A是SO 2，N，CH，CH 2，CHCH 3，C = O，C = S，C-SCH 3，C = NH，C-NH 2，C-NHCH 3，C-NHCOOCH 3或C-NHCN。 B是CH 2，CH，C = O，N，NH或N-CH 3; n为0或1; 且D为CH，CH 2，C = O，O，N，NH或N-CH 3。这些新化合物适用于治疗精神分裂症，帕金森病，焦虑症，抑郁症或作为降低动物或人类宿主血压的化合物。

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