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1. 发明授权

US06232313B1 Pyridazino quinoline compounds 失效
标题翻译：哒嗪喹啉化合物
公开(公告)号：US06232313B1
公开(公告)日：2001-05-15
申请号：US09044109
申请日：1998-03-19
申请人： Thomas Michael Bare , Timothy Wayne Davenport , James Roy Empfield , Jeffrey Alan McKinney , Richard Bruce Sparks
发明人： Thomas Michael Bare , Timothy Wayne Davenport , James Roy Empfield , Jeffrey Alan McKinney , Richard Bruce Sparks
IPC分类号： A61K315025
CPC分类号： C07D471/04 , C07D215/56
摘要： The present invention relates to compounds, pharmaceutical compositions and methods of using compounds having the formula below in the treatment and prevention of certain diseases or conditions. Where the ring designated A is chosen from ortho substituted aryl or heteroaryl species, R1 and R2 are chosen independently from —(CH2)nL where L is selected from a variety of substituents including hydrogen, and aryl, heteroaryl or heterocyclic groups and R4 is chosen from a variety of substituents including halogen and alkyl groups. The compounds are useful in treating and preventing neurological disorders associated with excitatory amino acids.
摘要翻译：本发明涉及在治疗和预防某些疾病或病症时使用具有下式的化合物的化合物，药物组合物和方法。当指定为A的环选自邻位取代的芳基或杂芳基时，R 1和R 2独立地选自 - （CH 2）n L，其中L选自多种取代基，包括氢和芳基，杂芳基或杂环基，并且选择R4 来自各种取代基，包括卤素和烷基。该化合物可用于治疗和预防与兴奋性氨基酸相关的神经障碍。

2. 发明授权

US6103721A Heteroaryl-substituted pyridazino quinoline compounds 失效
标题翻译：杂芳基取代的哒嗪喹啉化合物
公开(公告)号：US6103721A
公开(公告)日：2000-08-15
申请号：US455096
申请日：1999-12-06
申请人： Thomas Michael Bare , Timothy Wayne Davenport , James Roy Empfield , Jeffrey Alan McKinney , Richard Bruce Sparks
发明人： Thomas Michael Bare , Timothy Wayne Davenport , James Roy Empfield , Jeffrey Alan McKinney , Richard Bruce Sparks
IPC分类号： A61K31/50 , A61K31/5025 , A61P3/08 , A61P3/10 , A61P9/10 , A61P25/00 , A61P25/08 , A61P25/28 , A61P43/00 , C07D215/56 , C07D221/00 , C07D221/04 , C07D237/00 , C07D471/04 , C07D471/14 , C07D495/14
CPC分类号： C07D471/04 , C07D215/56
摘要： The present invention concerns compounds according to the following formula, ##STR1## wherein: R.sup.1 is (CH.sub.2).sub.n,L where n is an integer in the range 0 to 6, and L is a carbon-linked five-membered heteroaryl ring having an oxygen or sulfur heteroatom, R.sup.4 is hydrogen, halo or NO.sub.2, and pharmaceutical compositions and methods of using thereof in the treatment and/or prevention of neurological diseases or conditions.
摘要翻译：本发明涉及根据下式的化合物，其中：R1是（CH2）n，L，其中n是0-6的整数，L是具有氧或硫的碳连接的五元杂芳基环杂原子，R4是氢，卤素或NO2，以及其用于治疗和/或预防神经疾病或病症的药物组合物和方法。

3. 发明授权

US06214826B1 Pyridazino quinoline compounds 失效
标题翻译：哒嗪喹啉化合物
公开(公告)号：US06214826B1
公开(公告)日：2001-04-10
申请号：US09365562
申请日：1999-08-02
申请人： Thomas Michael Bare , Marc Jerome Chapdelaine , Timothy Wayne Davenport , James Roy Empfield , Laura Enid Garcia-Davenport , Paul Francis Jackson , Jeffrey Alan McKinney , Charles David McLaren , Richard Bruce Sparks
发明人： Thomas Michael Bare , Marc Jerome Chapdelaine , Timothy Wayne Davenport , James Roy Empfield , Laura Enid Garcia-Davenport , Paul Francis Jackson , Jeffrey Alan McKinney , Charles David McLaren , Richard Bruce Sparks
IPC分类号： A61K315025
CPC分类号： C07D471/04
摘要： The invention relates to pyridazinoquinoline compounds of the formulas B and B′ wherein Ring A is selected from an ortho fused aromatic or heteroaromatic five- or six-membered ring and R1, R3 and R4 are substituents selected from halo, OH, OCF3, NO2, CN, NR′R″, SO2NR′R″, SOmR′alkyl, and a variety of alkyl, aryl, heterocyclic and heteroaryl groups, to pharmaceutical compositions containing them and to methods utilizing them for the treatment of neurological disorders.
摘要翻译：本发明涉及式B和B'的哒嗪喹啉化合物，其中环A选自邻稠合芳族或杂芳族五元或六元环，且R 1，R 3和R 4为选自卤素，OH，OCF 3，NO 2， CN，NR'R“，SO2NR'R”，SOmR'烷基，以及各种烷基，芳基，杂环和杂芳基，含有它们的药物组合物以及利用它们用于治疗神经障碍的方法。

4. 发明授权

US5837705A Alpha-substituted pyridazino quinoline compounds 失效
标题翻译： α-取代哒嗪喹啉化合物
公开(公告)号：US5837705A
公开(公告)日：1998-11-17
申请号：US617728
申请日：1996-04-01
申请人： Thomas Michael Bare , James Roy Empfield , Janet Marie Forst , Keith John Herzog , Richard Bruce Sparks
发明人： Thomas Michael Bare , James Roy Empfield , Janet Marie Forst , Keith John Herzog , Richard Bruce Sparks
IPC分类号： C07D491/147 , A61K31/50 , A61P25/00 , A61P25/04 , A61P25/28 , A61P25/30 , C07D471/04 , C07D471/14 , C07D495/14 , C07D491/14
CPC分类号： C07D471/04
摘要： The invention relates to alpha-substituted pyridazino-quinoline compounds of the formula I: ##STR1## wherein Ring A is chosen from an ortho fused aromatic or heteroaromatic five- or six-membered ring; R.sup.1 is selected from a variety of substituents including halogen, (1-4C)alkyl and nitro; R.sup.2 is selected from a group of the formula R2', R2" or R2"' wherein R2' is --CHR.sup.3 (CH.sub.2).sub.n C(O)NR.sup.5 R.sup.6 ; R2" is --CHR.sup.3 (CH.sub.2).sub.n R.sup.4 and R2"' is --CHR.sup.3 (CH.sub.2).sub.n L wherein n is 0-6; R.sup.5 is aryl or substituted aryl; R.sup.6 is (1-6C)alkyl or hydrogen; R.sup.3 is (1-6C)alkyl, (0-6C)alkylCF.sub.3 or (0-6C)alkylCOOR'; R.sup.4 is (1-6C)alkyl, (2-6C)alkyl containing a double or triple bond, or (0-6C)alkylaryl; L is a variety of substituents including phenyl, heteroaryl and CO.sub.2 R'; R' is hydrogen or (1-4C)alkyl; Z is selected from oxo, --OH, H,H--, H, (1-6C)alkyl or (1-6C)alkylaryl; and R.sup.7 is hydrogen or --(CO)R.sup.8 wherein R.sup.8 is a variety of substituents including hydrogen and (1-12C) alkyl.
摘要翻译：本发明涉及式I的α-取代的哒嗪 - 喹啉化合物：其中环A选自邻近稠合芳族或杂芳族五元或六元环; R1选自多种取代基，包括卤素，（1-4C）烷基和硝基; R2选自式R2'，R2“或R2”'的基团，其中R2'为-CHR3（CH2）nC（O）NR5R6; R2“是-CHR3（CH2）nR4，R2”'是-CHR3（CH2）nL，其中n是0-6; R5是芳基或取代的芳基; R6是（1-6C）烷基或氢; R3是（1-6C）烷基，（0-6C）烷基CF3或（0-6C）烷基COOR'; R4是（1-6C）烷基，含有双键或三键的（2-6C）烷基，或（0-6C）烷基芳基; L是各种取代基，包括苯基，杂芳基和CO 2 R'; R'是氢或（1-4C）烷基; Z选自氧代，-OH，H，H，H，（1-6C）烷基或（1-6C）烷基芳基; 并且R 7是氢或 - （CO）R 8，其中R 8是各种取代基，包括氢和（1-12C）烷基。

5. 发明授权

US5693639A Therapeutic heterocyclyl amionosulfonyl phenyl compounds 失效
标题翻译：治疗性杂环酰胺基磺酰基苯基化合物
公开(公告)号：US5693639A
公开(公告)日：1997-12-02
申请号：US604064
申请日：1996-02-20
申请人： James Roy Empfield , Daniel Ray Mayhugh , Keith Russell
发明人： James Roy Empfield , Daniel Ray Mayhugh , Keith Russell
IPC分类号： A61K31/18 , A61K31/40 , A61K31/415 , A61K31/44 , A61K31/445 , A61K31/535 , A61K31/5375 , A61K31/54 , A61K31/63 , A61K31/635 , A61P13/02 , A61P15/00 , C07C311/16 , C07C311/21 , C07C311/29 , C07C311/39 , C07C311/44 , C07C311/46 , C07C323/67 , C07D213/76 , C07D233/56 , C07D249/12 , C07D295/22 , C07D295/26 , C07D401/02
CPC分类号： C07D295/26 , C07C311/29 , C07C311/46
摘要： Compounds of formula I ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and A-B have any of the meanings given in the specification, and their pharmaceutically acceptable salts are useful in the treatment of urinery incontinence. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.
摘要翻译：式I的化合物其中R1，R2，R3，R4，R5和A-B具有本说明书中给出的任何含义及其药学上可接受的盐可用于治疗尿失禁。还公开了药物组合物，制备式I化合物和中间体的方法。

6. 发明授权

US06737424B2 Alpha-substituted pyridazino quinoline compounds 失效
标题翻译： α-取代哒嗪喹啉化合物
公开(公告)号：US06737424B2
公开(公告)日：2004-05-18
申请号：US09192713
申请日：1998-11-16
申请人： Thomas Michael Bare , James Roy Empfield , Janet Marie Forst , Keith John Herzog , Richard Bruce Sparks
发明人： Thomas Michael Bare , James Roy Empfield , Janet Marie Forst , Keith John Herzog , Richard Bruce Sparks
IPC分类号： A61K315025
CPC分类号： C07D471/04
摘要： Alpha-substituted pyridazino-quinoline compounds of formula Ia useful for the treatment of strokes and neurodegenerative disorders: wherein R1 is selected from a variety of substituents including halogen, (C1-C4)alkyl and nitro; R2 is selected from cycloalkyl moieties of 5-7 carbon atoms and the groups R2′ and R2″ as defined in the specification, a dashed bond indicates a single or double bond, and R7 is selected from H and CO(C1-C3)alkyl.
摘要翻译：可用于治疗中风和神经变性疾病的式Ia的α-取代的哒嗪 - 喹啉化合物：其中R 1选自多种取代基，包括卤素，（C 1 -C 4）烷基和硝基; R 2选自5-7个碳原子的环烷基部分和如说明书中定义的基团R 2'和R 2“，虚键表示单键或双键，并且R 7选自H和 CO（C 1 -C 3）烷基。

7. 发明授权

US5900432A Therapeutic N-(4-benzoyl-2-methyl-phenyl)-3,3,3-trifluoro-2-hydroxy-2-methyl-propana mides 失效
标题翻译：治疗性N-（4-苯甲酰基-2-甲基 - 苯基）-3,3,3-三氟-2-羟基-2-甲基 - 丙酰胺
公开(公告)号：US5900432A
公开(公告)日：1999-05-04
申请号：US542114
申请日：1995-10-12
申请人： James Roy Empfield , Cyrus John Ohnmacht , Keith Russell , Diane Amy Trainor , Paul James Warwick, Jr.
发明人： James Roy Empfield , Cyrus John Ohnmacht , Keith Russell , Diane Amy Trainor , Paul James Warwick, Jr.
IPC分类号： A61K31/165 , A61K31/275 , A61K31/44 , A61K31/4409 , A61P13/02 , A61P15/00 , C07C233/75 , C07C235/16 , C07C255/49 , C07C255/60 , C07C317/40 , C07D213/71 , C07D237/14 , C07D237/18 , C07D237/20 , C07D239/34 , C07D239/38 , C07D239/42 , C07D241/18 , C07D241/20 , A61K31/16 , C07C51/255 , C07C233/01 , C07C237/20
CPC分类号： C07C235/16 , C07C255/60 , C07C317/40 , C07D213/71
摘要： Compounds of formula I: ##STR1## wherein, ring C, A--B, R.sup.1, n, R.sup.2, and R.sup.3 have any of the meanings given in the specification, and their pharmaceutically acceptable salts are useful in the treatment of urinery incontinence. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.
摘要翻译：式I化合物：其中环C，A-B，R 1，n，R 2和R 3具有说明书中给出的任何含义，并且其药学上可接受的盐可用于治疗尿失禁。还公开了药物组合物，制备式I化合物和中间体的方法。

8. 发明授权

US5744471A Pyridazion quinoline compounds 失效
标题翻译：哒嗪喹啉化合物
公开(公告)号：US5744471A
公开(公告)日：1998-04-28
申请号：US637641
申请日：1996-04-17
申请人： Thomas Michael Bare , Timothy Wayne Davenport , James Roy Empfield , Jeffrey Alan McKinney , Richard Bruce Sparks
发明人： Thomas Michael Bare , Timothy Wayne Davenport , James Roy Empfield , Jeffrey Alan McKinney , Richard Bruce Sparks
IPC分类号： A61K31/50 , A61K31/5025 , A61P3/08 , A61P3/10 , A61P9/10 , A61P25/00 , A61P25/08 , A61P25/28 , A61P43/00 , C07D215/56 , C07D221/00 , C07D221/04 , C07D237/00 , C07D471/04 , C07D471/14 , C07D495/14 , C07D491/14
CPC分类号： C07D471/04 , C07D215/56
摘要： The present invention relates to compounds, pharmaceutical compositions and methods of using compounds of formula (I) in the treatment and/or prevention of certain diseases or conditions. In formula (I), A is chosen from ortho substituted aryl or heteroaryl species, X is chosen from --OH, --SH, NHR and R.sup.1 or R.sup.2 is chosen from --(CH.sub.2).sub.n L wherein L may be selected from a variety of substituents including aryl, heteroaryl and heterocyclic groups. The compounds are useful in treating and/or preventing neurological disorders associated with excitatory amino acids. ##STR1##
摘要翻译： PCT No.PCT / GB94 / 02295 371日期：1996年4月17日 102（e）日期1996年4月17日PCT 1994年10月20日PCT公布。出版物WO95 / 11244 日期1995年04月27日本发明涉及使用式（I）化合物治疗和/或预防某些疾病或病症的化合物，药物组合物和方法。在式（I）中，A选自邻位取代的芳基或杂芳基，X选自-OH，-SH，NHR，R 1或R 2选自 - （CH 2）n L，其中L可以选自多种取代基包括芳基，杂芳基和杂环基。该化合物可用于治疗和/或预防与兴奋性氨基酸相关的神经障碍。我

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