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1. 发明授权

US6046239A Anthranilic acid analogs 失效
标题翻译：邻氨基苯甲酸类似物
公开(公告)号：US6046239A
公开(公告)日：2000-04-04
申请号：US128493
申请日：1998-08-03
申请人： Joseph Richard Lennox , Schuyler Adam Antane , John Anthony Butera
发明人： Joseph Richard Lennox , Schuyler Adam Antane , John Anthony Butera
IPC分类号： A61K31/192 , A61K31/27 , A61K31/455 , A61K31/195
CPC分类号： A61K31/27 , A61K31/192 , A61K31/455
摘要： Compounds of the formula: ##STR1## wherein: R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7 and R.sub.8 are, independently, hydrogen, COOR.sub.15, halogen, nitro, cyano, C.sub.1-10 alkoxy, C.sub.1-10 haloalkoxy, sulfonic acid, C.sub.1-10 alkylsulfonyl, C.sub.6-12 arylsulfonyl, C.sub.6-12 aralkylsulfonyl, C.sub.1-10 alkylsulfinyl, C.sub.6-12 alkylsulfinyl, C.sub.6-12 aralkylsulfinyl, sulfamoyl, C.sub.1-10 alkylsulfamido, C.sub.6-12 alkylsulfamido, C.sub.1-10 alkanoyl, C.sub.6-12 aryloyl, C.sub.6-12 aralkanoyl, amino, C.sub.1-10 alkylamino, C.sub.2-10 dialkylamino, C.sub.6-12 aralkylamino, C.sub.6-12 arylamino, carboxamido, C.sub.1-10 alkylcarboxamido, C.sub.6-12 arylcarboxamido, C.sub.1-10 haloalkyl, C.sub.1-10 alkyl, C.sub.2-12 alkenyl, C.sub.6-12 aryl, C.sub.6-12 aralkyl; with the proviso that at least one of R.sub.4 and R.sub.5 is COOR.sub.15 ;R.sub.9 is hydrogen, C.sub.1-10 alkyl and C.sub.1-10 haloalkyl;R.sub.10 is hydrogen, C.sub.1-10 alkyl, C.sub.1-10 haloalkyl, or C.sub.2-12 alkylidene;R.sub.15 is hydrogen, metal cation, acetylamido, alkoxyacetoyl or a related moiety which delivers the carboxylate in vivo;the dotted line is an optional double bond; with the proviso that when R.sub.10 is an alkylidene moiety, the double bond is absent; andW is nitrogen or carbon bearing a hydrogen, or R.sub.4, R.sub.5 or R.sub.6 as hereinbefore defined; or pharmaceutical salts thereof, are useful in the treatment of disorders associated with smooth muscle contraction via potassium channel and chloride channel modulation.
摘要翻译：下式的化合物：其中：R 1，R 2，R 3，R 4，R 5，R 6，R 7和R 8独立地是氢，COOR 15，卤素，硝基，氰基，C 1-10烷氧基，C 1-10卤代烷氧基，磺酸，C 1 -10烷基磺酰基，C6-12芳基磺酰基，C6-12芳烷基磺酰基，C1-10烷基亚磺酰基，C6-12烷基亚磺酰基，C6-12芳烷基亚磺酰基，氨磺酰基，C1-10烷基磺酰氨基，C6-12烷基磺酰氨基，C1-10烷酰基，C6-12芳基，C 6-12芳烷酰基，氨基，C 1-10烷基氨基，C 2-10二烷基氨基，C 6-12芳烷基氨基，C 6-12芳基氨基，甲酰氨基，C 1-10烷基羧酰氨基，C 6-12芳基羧酰胺基，C 1-10卤代烷基，C 1-10烷基， C2-12烯基，C6-12芳基，C6-12芳烷基; 条件是R4和R5中的至少一个是COOR15; R9是氢，C1-10烷基和C1-10卤代烷基; R10是氢，C1-10烷基，C1-10卤代烷基或C2-12亚烷基; R15是氢，金属阳离子，乙酰氨基，烷氧基乙酰基或在体内递送羧酸盐的相关部分; 虚线是可选的双键; 条件是当R 10是亚烷基部分时，双键不存在; 并且W是带有氢的氮或碳，或如上文所定义的R4，R5或R6; 或其药用盐可用于治疗通过钾通道和氯化物通道调节与平滑肌收缩相关的病症。

2. 发明申请

US20100168194A1 Amino-5-[4-(difluoromethoxy)phenyl]-5-phenylimidazolone Compounds For The Inhibition Of Beta-secretase 审中-公开
标题翻译：氨基-5- [4-（二氟甲氧基）苯基] -5-苯基咪唑酮化合物抑制β-分泌酶
公开(公告)号：US20100168194A1
公开(公告)日：2010-07-01
申请号：US12721086
申请日：2010-03-10
申请人： Michael Sotirios Malamas , Albert Jean Robichaud , Alexander Michael Porte , Koi Michele Morris , William R. Solvibile , Ji-In Kim , Schuyler Adam Antane
发明人： Michael Sotirios Malamas , Albert Jean Robichaud , Alexander Michael Porte , Koi Michele Morris , William R. Solvibile , Ji-In Kim , Schuyler Adam Antane
IPC分类号： A61K31/4166 , C07D233/30 , A61P25/28
CPC分类号： C07D233/70 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12
摘要： The present invention provides compounds and methods for the use thereof to inhibit β-secretase (BACE) and treat β-amyloid deposits and neurofibrillary tangles.
摘要翻译：本发明提供了用于抑制和分泌（BACE）和治疗和淀粉样沉积物和神经原纤维缠结的化合物和方法。

3. 发明授权

US07585873B2 1-(aminoalkyl)-3-sulfonylazaindoles as 5-hydroxytryptamine-6 ligands 失效
标题翻译： 1-（氨基烷基）-3-磺酰基嘧啶，为5-羟基色胺-6配体
公开(公告)号：US07585873B2
公开(公告)日：2009-09-08
申请号：US11367620
申请日：2006-03-03
申请人： Ronald Charles Bernotas , Steven Edward Lenicek , Schuyler Adam Antane
发明人： Ronald Charles Bernotas , Steven Edward Lenicek , Schuyler Adam Antane
IPC分类号： A61K31/437 , A61K31/5377
CPC分类号： C07D519/04 , A61K31/4745 , A61K31/519 , C07D471/04 , C07D519/00
摘要： The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor.
摘要翻译：本发明提供式I化合物及其用于治疗与5-HT 6受体有关或受其影响的病症的用途。

4. 发明授权

US07074792B2 1-(aminoalkyl)-3-sulfonylazaindoles as 5-hydroxytryptamine-6 ligands 失效
公开(公告)号：US07074792B2
公开(公告)日：2006-07-11
申请号：US10963132
申请日：2004-10-12
申请人： Ronald Charles Bernotas , Steven Edward Lenicek , Schuyler Adam Antane
发明人： Ronald Charles Bernotas , Steven Edward Lenicek , Schuyler Adam Antane
IPC分类号： A61K31/4985 , C07D487/04
CPC分类号： C07D519/04 , A61K31/4745 , A61K31/519 , C07D471/04 , C07D519/00
摘要： The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor.

5. 发明授权

US6127392A Anthranilic acid analogs 失效
标题翻译：邻氨基苯甲酸类似物
公开(公告)号：US6127392A
公开(公告)日：2000-10-03
申请号：US127753
申请日：1998-08-03
申请人： Joseph Richard Lennox , Schuyler Adam Antane , John Anthony Butera
发明人： Joseph Richard Lennox , Schuyler Adam Antane , John Anthony Butera
IPC分类号： A61K31/27 , A61K31/455 , C07C233/55 , A01N43/40 , A01N37/10 , C07C205/07 , C07C233/54
CPC分类号： A61K31/455 , A61K31/27 , C07C233/55
摘要： Compounds of the formula: wherein:R.sub.1, R.sub.2, R.sub.3, R.sub.4,R.sub.5, R.sub.6, R.sub.7 and R.sub.8 are, independently, hydrogen, COOR.sub.15, halogen, nitro, cyano, C.sub.1-10 alkoxy, C.sub.1-10 haloalkoxy, sulfonic acid, C.sub.1-10 alkylsulfonyl, C.sub.6-12 arylsulfonyl, C.sub.6-12 aralkylsulfonyl, C.sub.1-10 alkylsulfinyl, C.sub.6-12 arylsufinyl, C.sub.6-12 aralkylsulfinyl, sulfamoyl, C.sub.1-10 alkylsulfamido, C.sub.6-12 arylsulfamido, C.sub.1-10 alkanoyl, C.sub.6-12 aryloyl, C.sub.6-12 aralkanoyl, amino, C.sub.1-10 alkylamino, C.sub.2-10 dialkylamino, C.sub.6-12 aralkylamino, C.sub.6-12 arylamino, carboxamido, C.sub.1-10 alkylcarboxamido, C.sub.6-12 arylcarboxamido, C.sub.1-10 haloalkyl, C.sub.1-10 alkyl, C.sub.2-12 alkenyl, C.sub.6-12 aryl, C.sub.6-12 aralkyl; with the proviso that at least one of R.sub.4 and R.sub.5 is COOR.sub.15 ;R.sub.9 is hydrogen, C.sub.1-10 alkyl and C.sub.1-10 haloalkyl;R.sub.10 is hydrogen, C.sub.1-10 alkyl, C.sub.1-10 haloalkyl, or C.sub.2-12 alkylidene;R.sub.15 is hydrogen, metal cation, acetylamido, alkoxyacetoyl or a related moiety which delivers the carboxylate in vivo;the dotted line is an optional double bond; with the proviso that when R.sub.10 is an alkylidene moiety, the double bond is absent; andW is nitrogen or carbon bearing a hydrogen, or R.sub.4, R.sub.5 or R.sub.6 as hereinbefore defined; or pharmaceutcal salts thereof, are useful in the treatment of disorders associated with smooth muscle contraction via potassium channel and chloride channel modulation.
摘要翻译：下式的化合物：其中：R 1，R 2，R 3，R 4，R 5，R 6，R 7和R 8独立地是氢，COOR 15，卤素，硝基，氰基，C 1-10烷氧基，C 1-10卤代烷氧基，磺酸，C 1 -10烷基磺酰基，C6-12芳基磺酰基，C6-12芳烷基磺酰基，C1-10烷基亚磺酰基，C6-12芳基亚磺酰基，C6-12芳烷基亚磺酰基，氨磺酰基，C1-10烷基磺酰氨基，C6-12芳基磺酰氨基，C1-10烷酰基，C6-12芳基，C 6-12芳烷酰基，氨基，C 1-10烷基氨基，C 2-10二烷基氨基，C 6-12芳烷基氨基，C 6-12芳基氨基，甲酰氨基，C 1-10烷基羧酰氨基，C 6-12芳基羧酰胺基，C 1-10卤代烷基，C 1-10烷基， C2-12烯基，C6-12芳基，C6-12芳烷基; 条件是R4和R5中的至少一个是COOR15; R9是氢，C1-10烷基和C1-10卤代烷基; R10是氢，C1-10烷基，C1-10卤代烷基或C2-12亚烷基; R15是氢，金属阳离子，乙酰氨基，烷氧基乙酰基或在体内递送羧酸盐的相关部分; 虚线是可选的双键; 条件是当R 10是亚烷基部分时，双键不存在; 并且W是带有氢的氮或碳，或如上文所定义的R4，R5或R6; 或其药物盐可用于治疗通过钾通道和氯化物通道调节与平滑肌收缩相关的疾病。

6. 发明授权

US07723368B2 Amino-5-[4-(difluoromethoxy)phenyl]-5-phenylimidazolone compounds for the inhibition of beta-secretase 失效
标题翻译：用于抑制β-分泌酶的氨基-5- [4-（二氟甲氧基）苯基] -5-苯基咪唑啉酮化合物
公开(公告)号：US07723368B2
公开(公告)日：2010-05-25
申请号：US12053086
申请日：2008-03-21
申请人： Michael Sotirios Malamas , Albert Jean Robichaud , Alexander Michael Porte , Koi Michele Morris , William R. Solvibile , Ji-In Kim , Schuyler Adam Antane
发明人： Michael Sotirios Malamas , Albert Jean Robichaud , Alexander Michael Porte , Koi Michele Morris , William R. Solvibile , Ji-In Kim , Schuyler Adam Antane
IPC分类号： A61K31/4166 , A61K31/4168 , C07D233/30
CPC分类号： C07D233/70 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12
摘要： The present invention provides compounds and methods for the use thereof to inhibit β-secretase (BACE) and treat β-amyloid deposits and neurofibrillary tangles.
摘要翻译：本发明提供了用于抑制和分泌（BACE）和治疗和淀粉样沉积物和神经原纤维缠结的化合物和方法。

7. 发明申请

US20090036439A1 3-ARYL-4-HYDROXYFURANONE COMPOUNDS AND THE HUMAN AND ANIMAL HEALTH USE THEREOF 失效
标题翻译： 3-ARYL-4-HYDROXYFURANONE化合物及其人类和动物健康用途
公开(公告)号：US20090036439A1
公开(公告)日：2009-02-05
申请号：US12233709
申请日：2008-09-19
申请人： Craig Eugene Caufield , Schuyler Adam Antane , Koi Michele Morris , Shaughnessy McGrath Naughton , Dominick Anthony Quagliato , Patrick Michael Andrae , Annmarie Enos , John F. Chiarello
发明人： Craig Eugene Caufield , Schuyler Adam Antane , Koi Michele Morris , Shaughnessy McGrath Naughton , Dominick Anthony Quagliato , Patrick Michael Andrae , Annmarie Enos , John F. Chiarello
IPC分类号： A01N43/84 , C07D307/26 , A01N43/08 , C07D405/02 , A01N43/60 , A01N43/40 , C07D233/54 , A01N43/50 , C07D231/10 , A01N43/56 , C07D413/02 , A01P5/00
CPC分类号： C07D307/34 , A01N43/08 , A01N43/10 , A01N43/30 , A01N43/36 , A01N43/40 , A01N43/56 , A01N43/60 , A01N43/84 , A01N47/06 , C07D405/06 , C07D405/10 , C07D407/06 , C07D409/04 , C07D409/06 , C07D409/14
摘要： The present invention provides a compound of formula I and the use thereof for the inhibition of bacterial cell wall biosynthesis and for the therapeutic treatment of bacterial infection or disease in a patient in need thereof. The present invention also provides the use of the formula I compound for the control of ecto- or endoparasites in homeothermic animals.
摘要翻译：本发明提供式I化合物及其用于抑制细菌细胞壁生物合成和用于治疗有需要的患者的细菌感染或疾病的用途。本发明还提供式I化合物用于控制恒温动物体内外寄生虫或内寄生虫的用途。

8. 发明申请

US20090012139A1 AMINO-5-[4-(DIFLUOROMETHOXY) PHENYL]-5-PHENYLIMIDAZOLONE COMPOUNDS FOR THE INHIBITION OF BETA-SECRETASE 审中-公开
标题翻译：氨基-5- [4-（二氟甲基）苯基] -5-苯基咪唑烷酮化合物用于抑制β-分泌酶
公开(公告)号：US20090012139A1
公开(公告)日：2009-01-08
申请号：US12201026
申请日：2008-08-29
申请人： Michael Sotirios MALAMAS , James Joseph ERDEI , William Floyd FOBARE , Dominick Anthony QUAGLIATO , Schuyler Adam ANTANE , Albert Jean ROBICHAUD
发明人： Michael Sotirios MALAMAS , James Joseph ERDEI , William Floyd FOBARE , Dominick Anthony QUAGLIATO , Schuyler Adam ANTANE , Albert Jean ROBICHAUD
IPC分类号： C07D233/88 , A61K31/4168 , A61P25/00 , A61P25/28
CPC分类号： C07D233/88 , C07D401/12 , C07D409/12
摘要： The present invention provides a 2-amino-5-[4-(difluoromethoxy)phenyl]-5-phenylimidazolone compound of formula I The present invention also provides methods for the use thereof to inhibit β-secretase (BACE) and treat β-amyloid deposits and neurofibrillary tangles.
摘要翻译：本发明提供式I的2-氨基-5- [4-（二氟甲氧基）苯基] -5-苯基咪唑酮化合物本发明还提供了用于抑制β-分泌酶（BACE）和治疗β-淀粉样蛋白的方法沉积物和神经原纤维缠结。

9. 发明授权

US07423158B2 Amino-5-[4-(difluoromethoxy)phenyl]-5-phenylimidazolone compounds for the inhibition of β-secretase 失效
标题翻译：用于抑制β-分泌酶的氨基-5- [4-（二氟甲氧基）苯基] -5-苯基咪唑啉酮化合物
公开(公告)号：US07423158B2
公开(公告)日：2008-09-09
申请号：US11526511
申请日：2006-09-25
申请人： Michael Sotirios Malamas , James Joseph Erdei , William Floyd Fobare , Dominick Anthony Quagliato , Schuyler Adam Antane , Albert Jean Robichaud
发明人： Michael Sotirios Malamas , James Joseph Erdei , William Floyd Fobare , Dominick Anthony Quagliato , Schuyler Adam Antane , Albert Jean Robichaud
IPC分类号： A61K31/4168 , C07D233/44
CPC分类号： C07D233/88 , C07D401/12 , C07D409/12
摘要： The present invention provides a 2-amino-5-[4-(difluoromethoxy)phenyl]-5-phenylimidazolone compound of formula I The present invention also provides methods for the use thereof to inhibit β-secretase (BACE) and treat β-amyloid deposits and neurofibrillary tangles.
摘要翻译：本发明提供式I的2-氨基-5- [4-（二氟甲氧基）苯基] -5-苯基咪唑酮化合物本发明还提供了用于抑制β-分泌酶（BACE）和治疗β-淀粉样蛋白的方法沉积物和神经原纤维缠结。

10. 发明授权

US07666904B2 3-aryl-4-hydroxyfuranone compounds and the human and animal health use thereof 失效
标题翻译： 3-芳基-4-羟基呋喃酮化合物及其人和动物健康用途
公开(公告)号：US07666904B2
公开(公告)日：2010-02-23
申请号：US12233709
申请日：2008-09-19
申请人： Craig Eugene Caufield , Schuyler Adam Antane , Koi Michele Morris , Shaughnessy McGrath Naughton , Dominick Anthony Quagliato , Patrick Michael Andrae , Annmarie Enos , John F. Chiarello
发明人： Craig Eugene Caufield , Schuyler Adam Antane , Koi Michele Morris , Shaughnessy McGrath Naughton , Dominick Anthony Quagliato , Patrick Michael Andrae , Annmarie Enos , John F. Chiarello
IPC分类号： A61K31/341 , C07D307/60
CPC分类号： C07D307/34 , A01N43/08 , A01N43/10 , A01N43/30 , A01N43/36 , A01N43/40 , A01N43/56 , A01N43/60 , A01N43/84 , A01N47/06 , C07D405/06 , C07D405/10 , C07D407/06 , C07D409/04 , C07D409/06 , C07D409/14
摘要： The present invention provides a compound of formula I and the use thereof for the inhibition of bacterial cell wall biosynthesis and for the therapeutic treatment of bacterial infection or disease in a patient in need thereof. The present invention also provides the use of the formula I compound for the control of ecto- or endoparasites in homeothermic animals.
摘要翻译：本发明提供式I化合物及其用于抑制细菌细胞壁生物合成和用于治疗有需要的患者的细菌感染或疾病的用途。本发明还提供式I化合物用于控制恒温动物体内外寄生虫或内寄生虫的用途。

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