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公开(公告)号：US08778946B2
公开(公告)日：2014-07-15
申请号：US13882765
申请日：2011-11-17
IPC分类号： C07D471/04 , A61K31/496 , C07D487/04
CPC分类号： C07D487/04 , C07D471/04
摘要： The invention provides certain 3-substituted-6-(pyridinylmethoxy)-pyrrolopyridine compounds, particularly compounds of formula I and pharmaceutical compositions thereof. The invention further provides methods of using a compound of formula I to treat Parkinsons disease Formula (I).
摘要翻译： 本发明提供某些3-取代-6-（吡啶基甲氧基） - 吡咯并吡啶化合物，特别是式I化合物及其药物组合物。 本发明进一步提供使用式I化合物治疗帕金森病公式（I）的方法。
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公开(公告)号：US20130225602A1
公开(公告)日：2013-08-29
申请号：US13882765
申请日：2011-11-17
IPC分类号： C07D487/04
CPC分类号： C07D487/04 , C07D471/04
摘要： The invention provides certain 3-substituted-6-(pyridinylmethoxy)-pyrrolopyridine compounds, particularly compounds of formula I and pharmaceutical compositions thereof. The invention further provides methods of using a compound of formula I to treat Parkinsons disease Formula (I).
摘要翻译： 本发明提供某些3-取代-6-（吡啶基甲氧基） - 吡咯并吡啶化合物，特别是式I化合物及其药物组合物。 本发明进一步提供使用式I化合物治疗帕金森病公式（I）的方法。
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公开(公告)号：US07354920B2
公开(公告)日：2008-04-08
申请号：US10524921
申请日：2003-08-18
申请人： Manuel Javier Cases-Thomas , Helen Louise Haughton , Robin George Simmonds , Hélène Catherine Eugénie Rudyk , Magnus Wilhelm Walter , Sivi Ouwerkerk-Mahadevan , John Joseph Masters , Carlos Lamas-Peteira
发明人： Manuel Javier Cases-Thomas , Helen Louise Haughton , Robin George Simmonds , Hélène Catherine Eugénie Rudyk , Magnus Wilhelm Walter , Sivi Ouwerkerk-Mahadevan , John Joseph Masters , Carlos Lamas-Peteira
IPC分类号： A61K31/5375 , C07D265/30
CPC分类号： C07D265/30 , C07D413/10
摘要： Compounds of formula (I) wherein Rx is H; Ry is H or C1-C4 alkyl; each Rz is independently H or C1-C4 alkyl; X represents O; Y represents OH or OR; R is C1-C4 alkyl; and Ar1 and Ar2 are optionally substituted phenyl or 5- or 6-membered heteroaryl rings are selective inhibitors of the reuptake of norepinephrine.
摘要翻译： 其中Rx是H的式（I）化合物; R y为H或C 1 -C 4烷基; 每个R z独立地为H或C 1 -C 4烷基; X表示O; Y表示OH或OR; R是C 1 -C 4烷基; 和Ar 1和Ar 2是任选取代的苯基或5-或6-元杂芳环是去甲肾上腺素再摄取的选择性抑制剂。
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公开(公告)号：US07335660B2
公开(公告)日：2008-02-26
申请号：US10496535
申请日：2002-12-06
申请人： Javier Agejas-Chicharro , Graham Henry Timms , Andrew Caerwyn Williams , Nicholas Paul Camp , Jeremy Gilmore , Ana Belen Bueno Melendo , Carlos Lamas-Peteira
发明人： Javier Agejas-Chicharro , Graham Henry Timms , Andrew Caerwyn Williams , Nicholas Paul Camp , Jeremy Gilmore , Ana Belen Bueno Melendo , Carlos Lamas-Peteira
IPC分类号： A61K31/496 , C07D311/76 , C07D405/06 , C07D409/12 , C07D413/12 , C07D413/06 , C07D413/14 , C07D413/04 , C07D407/06 , C07D409/14 , C07D405/04 , C07D417/12 , C07D405/12
CPC分类号： C07D405/06 , C07D307/87 , C07D311/76 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/04
摘要： This invention relates to compounds of formula (I) where R1 to R12, —W—V—, —X—Y—, p and n have the values defined in claim 1, their preparation and use as pharmaceuticals for the treatment of central nervous system disorders, such as depression, bipolar disorder, and anxiety.
摘要翻译： 本发明涉及其中R 1至R 12，-WV-，-XY-，p和n具有权利要求1中定义的值的式（I）化合物， 其制备和用作药物用于治疗中枢神经系统疾病，例如抑郁症，双相性精神障碍和焦虑症。
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公开(公告)号：US20070060585A1
公开(公告)日：2007-03-15
申请号：US10575469
申请日：2004-12-10
IPC分类号： A61K31/5377 , A61K31/5375 , C07D413/02
CPC分类号： C07D265/30 , C07D295/027 , C07D295/192 , C07D401/10
摘要： Compounds of the general formula (I) are inhibitors of the reuptake of norepinephrine. As such, they may be useful for the treatment of disorders of the central and/or peripheral nervous system.
摘要翻译： 通式（I）的化合物是去甲肾上腺素再摄取的抑制剂。 因此，它们可用于治疗中枢和/或周围神经系统的病症。
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公开(公告)号：US06846830B2
公开(公告)日：2005-01-25
申请号：US10221822
申请日：2001-03-19
IPC分类号： A61K31/095 , A61K31/235 , A61K31/277 , A61K31/424 , A61K31/426 , A61K31/44 , A61K31/4409 , A61K31/505 , A61P25/08 , A61P43/00 , C07D213/06 , C07D213/127 , C07D213/16 , C07D213/26 , C07D213/30 , C07D213/32 , C07D213/57 , C07D213/61 , C07D213/68 , C07D239/26 , C07D277/24 , C07D213/02 , A61K31/445
CPC分类号： A61K31/095 , A61K31/235 , A61K31/277 , A61K31/426 , A61K31/44 , A61K31/4409 , A61K31/505 , C07D213/06 , C07D213/16 , C07D213/26 , C07D213/30 , C07D213/32 , C07D213/57 , C07D213/61 , C07D213/68 , C07D239/26 , C07D277/24
摘要： Use of compounds of the formula (I) where A, E, R1, R2, p and q have the meanings given in the specification are GluR6 antagonists useful for the treatment of disorders of the central nervous system.
摘要翻译： 其中A，E，R 1，R 2，p和q具有本说明书中给出的含义的式（I）化合物的用途是可用于治疗中枢神经系统疾病的GluR6拮抗剂。
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公开(公告)号：US07595315B2
公开(公告)日：2009-09-29
申请号：US10575469
申请日：2004-12-10
IPC分类号： A61K31/5375 , C07D265/30
CPC分类号： C07D265/30 , C07D295/027 , C07D295/192 , C07D401/10
摘要： Compounds of the general formula (I) are inhibitors of the reuptake of norepinephrine. As such, they may be useful for the treatment of disorders of the central and/or peripheral nervous system.
摘要翻译： 通式（I）的化合物是去甲肾上腺素再摄取的抑制剂。 因此，它们可用于治疗中枢和/或周围神经系统的病症。
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公开(公告)号：US20070276138A1
公开(公告)日：2007-11-29
申请号：US11637223
申请日：2006-12-11
申请人： Dawn Brooks , Alan Warshawsky , Chahrzad Montrose-Rafezadeh , Anne Reifel-Miller , Lourdes Prieto , Isabel Rojo , Jose Martin , Maria Gonzales Garcia , Alicia Torrado , Rafael Crespo , Carlos Lamas-Peteira , Robert Ardecky , Maria Finger
发明人： Dawn Brooks , Alan Warshawsky , Chahrzad Montrose-Rafezadeh , Anne Reifel-Miller , Lourdes Prieto , Isabel Rojo , Jose Martin , Maria Gonzales Garcia , Alicia Torrado , Rafael Crespo , Carlos Lamas-Peteira , Robert Ardecky , Maria Finger
IPC分类号： C07D265/30 , C07C233/87 , C07D207/02 , C07D209/04 , C07D209/32 , C07D211/40 , C07D277/62 , C07D307/87 , C07D317/06 , C07D333/76 , C07D333/08 , C07D333/02 , C07D317/70 , C07D311/30 , C07D307/02 , C07D215/20 , C07D217/02 , C07D233/02 , C07D241/04 , C07D257/04
CPC分类号： C07D209/48 , C07C59/68 , C07C59/72 , C07C59/90 , C07C217/20 , C07C217/84 , C07C217/92 , C07C219/10 , C07C233/25 , C07C233/29 , C07C233/60 , C07C233/75 , C07C235/56 , C07C235/64 , C07C239/12 , C07C255/54 , C07C2601/08 , C07D209/08 , C07D213/30 , C07D215/14 , C07D217/02 , C07D231/12 , C07D233/56 , C07D249/08 , C07D257/04 , C07D277/64 , C07D295/096 , C07D295/112 , C07D295/185 , C07D307/79 , C07D307/83 , C07D307/91 , C07D307/93 , C07D311/30 , C07D317/20 , C07D317/22 , C07D317/54 , C07D317/64 , C07D333/16 , C07D333/76 , C07D335/02
摘要： Disclosed is a compound represented by Structural Formula (I): Ar is a substituted or unsubstituted aromatic group. Q is a covalent bond, —CH2— or —CH2CH2—; W is a substituted or unsubstituted alkylene or a substituted or unsubstituted heteroalkylene linking group from two to ten atoms in length, preferably from two to seven atoms in length. Phenyl Ring A is optionally substituted with up to four substituents in addition to R1 and W. R1 is —(CH2)n—CH(OR2)—(CH2)mE, —(CH)═C(OR2)—(CH2)mE, —(CH2)n—CH(Y)—(CH2)mE or —(CH)═C(Y)—(CH2)mE; wherein E is COOR3, C1-C3-alkylnitrile, carboxamide, sulfonamide, acylsulfonamide or tetrazole and wherein sulfonamide, acylsulfonamide and tetrazole are optionally substituted with one or more substituents independently selected from: C1-C6 alkyl, haloalkyl and aryl-C0-4-alkyl; R2 is —H, an aliphatic group, a substituted aliphatic group, haloalkyl, an aromatic group, a substituted aromatic group, —COR4, —COOR4, —CONR5R6, —C(S)R4, —C(S)OR4 or —C(S)NR5R6. R3 is —H, an aliphatic group, a substituted aliphatic group, an aromatic group or a substituted aromatic group. Y is —O—, —CH2—, —CH2CH2— or —CH═CH— and is bonded to a carbon atom in Phenyl Ring A that is ortho to R1. R4-R6 are independently —H, an aliphatic group, a substituted aliphatic group, an aromatic group or a substituted aromatic group. n and m are independently 0, 1 or 2.
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公开(公告)号：US07192982B2
公开(公告)日：2007-03-20
申请号：US10479262
申请日：2002-05-30
申请人： Dawn Alisa Brooks , Alan M. Warshawsky , Chahrzad Montrose-Rafezadeh , Anne-Reifel Miller , Lourdes Prieto , Isabel Rojo , Jose Alfredo Martin , Maria Rosario Gonzales Garcia , Alicia Torrado , Rafael Ferritto Crespo , Carlos Lamas-Peteira , Robert J. Ardecky , Maria Martin-Ortega Finger
发明人： Dawn Alisa Brooks , Alan M. Warshawsky , Chahrzad Montrose-Rafezadeh , Anne-Reifel Miller , Lourdes Prieto , Isabel Rojo , Jose Alfredo Martin , Maria Rosario Gonzales Garcia , Alicia Torrado , Rafael Ferritto Crespo , Carlos Lamas-Peteira , Robert J. Ardecky , Maria Martin-Ortega Finger
CPC分类号： C07D209/48 , C07C59/68 , C07C59/72 , C07C59/90 , C07C217/20 , C07C217/84 , C07C217/92 , C07C219/10 , C07C233/25 , C07C233/29 , C07C233/60 , C07C233/75 , C07C235/56 , C07C235/64 , C07C239/12 , C07C255/54 , C07C2601/08 , C07D209/08 , C07D213/30 , C07D215/14 , C07D217/02 , C07D231/12 , C07D233/56 , C07D249/08 , C07D257/04 , C07D277/64 , C07D295/096 , C07D295/112 , C07D295/185 , C07D307/79 , C07D307/83 , C07D307/91 , C07D307/93 , C07D311/30 , C07D317/20 , C07D317/22 , C07D317/54 , C07D317/64 , C07D333/16 , C07D333/76 , C07D335/02
摘要： Disclosed is a compound represented by Structural Formula (I): Ar is a substituted or unsubstituted aromatic group. Q is a covalent bond, —CH2— or —CH2CH2—; W is a substituted or unsubstituted alkylene or a substituted or unsubstituted heteroalkylene linking group from two to ten atoms in length, preferably from two to seven atoms in length. Phenyl Ring A is optionally substituted with up to four substituents in addition to R1 and W, R1 is (CH2)n—CH(OR2)—(CH2)mE1, —(CH)═C(OR2)—(CH2)mE, —(CH2)n—CH(Y)—(CH2)mE or (CH)═C(Y)—(CH2)mE; wherein E is COOR3, C1–C3 alkylnitrile, carboxamide, sulfonamide, acylsulfonamide or tetrazole and wherein sulfonamide, acylsulfonamide and tetrazole are optionally substituted with one or more substituents independently selected from: C1–C6 alkyl, haloalkyl and aryl-C0-4-alkyl; R2 is H, an aliphatic group, a substituted aliphatic group, haloalkyl, an aromatic group, a substituted aromatic group, —COR4, —COOR4, —CONR5R6, —C(S)R4, —C(S)OR4 or C(S)NR5R6, R3 is H, an aliphatic group, a substituted aliphatic group, an aromatic group or a substituted aromatic group. Y is O—, CH2—, —CH2CH2— or CH═CH— and is bonded to a carbon atom in Phenyl Ring A that is ortho to R1. R4–R6 are independently H, an aliphatic group, a substituted aliphatic group, an aromatic group or a substituted aromatic group. n and m are independently 0, 1 or 2
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公开(公告)号：US20050020684A1
公开(公告)日：2005-01-27
申请号：US10479262
申请日：2002-05-30
申请人： Dawn Brooks , Alan Warshawsky , Chahrzad Montrose-Rafezadeh , Anne-Reifel Miller , Lourdes Prieto , Isabel Rojo , Jose Alfredo Martin , Maria Rosario Gonzales Garcia , Alicia Torrado , Rafael Crespo , Carlos Lamas-Peteira , Robert Ardecky , Maria Martin-Ortega Finger
发明人： Dawn Brooks , Alan Warshawsky , Chahrzad Montrose-Rafezadeh , Anne-Reifel Miller , Lourdes Prieto , Isabel Rojo , Jose Alfredo Martin , Maria Rosario Gonzales Garcia , Alicia Torrado , Rafael Crespo , Carlos Lamas-Peteira , Robert Ardecky , Maria Martin-Ortega Finger
IPC分类号： C07D295/08 , A61K31/19 , A61K31/275 , A61K31/343 , A61K31/352 , A61K31/353 , A61K31/36 , A61K31/381 , A61K31/40 , A61K31/4035 , A61K31/404 , A61K31/41 , A61K31/4164 , A61K31/428 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4453 , A61K31/47 , A61K31/472 , A61K31/495 , A61K31/5375 , A61K45/00 , A61P1/14 , A61P3/00 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/00 , A61P9/04 , A61P9/12 , A61P15/00 , C07B61/00 , C07C51/09 , C07C59/68 , C07C59/72 , C07C59/90 , C07C213/08 , C07C217/20 , C07C217/84 , C07C217/92 , C07C219/10 , C07C233/25 , C07C233/29 , C07C233/60 , C07C233/75 , C07C235/56 , C07C235/64 , C07C239/12 , C07C251/48 , C07C255/54 , C07D209/08 , C07D209/48 , C07D213/30 , C07D213/64 , C07D213/82 , C07D215/12 , C07D215/14 , C07D217/02 , C07D233/60 , C07D257/04 , C07D277/64 , C07D295/096 , C07D295/10 , C07D295/112 , C07D295/185 , C07D307/79 , C07D307/83 , C07D307/91 , C07D307/93 , C07D311/30 , C07D311/32 , C07D317/20 , C07D317/22 , C07D317/54 , C07D317/64 , C07D333/16 , C07D333/76 , C07D335/02 , C07D521/00 , C07F7/18 , A61K31/195 , C07C233/87
CPC分类号： C07D209/48 , C07C59/68 , C07C59/72 , C07C59/90 , C07C217/20 , C07C217/84 , C07C217/92 , C07C219/10 , C07C233/25 , C07C233/29 , C07C233/60 , C07C233/75 , C07C235/56 , C07C235/64 , C07C239/12 , C07C255/54 , C07C2601/08 , C07D209/08 , C07D213/30 , C07D215/14 , C07D217/02 , C07D231/12 , C07D233/56 , C07D249/08 , C07D257/04 , C07D277/64 , C07D295/096 , C07D295/112 , C07D295/185 , C07D307/79 , C07D307/83 , C07D307/91 , C07D307/93 , C07D311/30 , C07D317/20 , C07D317/22 , C07D317/54 , C07D317/64 , C07D333/16 , C07D333/76 , C07D335/02
摘要： Disclosed is a compound represented by Structural Formula (I): Ar is a substituted or unsubstituted aromatic group. Q is a covalent bond, —CH2— or —CH2CH2—; W is a substituted or unsubstituted alkylene or a substituted or unsubstituted heteroalkylene linking group from two to ten atoms in length, preferably from two to seven atoms in length. Phenyl Ring A is optionally substituted with up to four substituents in addition to R1 and W, R2 is (CH2)n—CH(OR2)—(CH2)nE, —(CH)═C(OR2)—(CH2)nE, —(CH2)n—CH(Y)—(CH2)mE or (CH)═C(Y)(CH2)mE; wherein E is COOR3, C1-C3 alkylnitrile, carboxamide, sulfonamide, acylsulfonamide or tetrazole and wherein sulfonamide, acylsulfonamide and tetrazole are optionally substituted with one or more substituents independently selected from: C1-C6 alkyl, haloalkyl and aryl-Co-4-alkyl; R2 is H, an aliphatic group, a substituted aliphatic group, haloalkyl, an aromatic group, a substituted aromatic group, —COR4, —COOR4, —CONR5R6, —C(S)R4, —C(S)OR4 or C(S)NR5R6, R3 is H, an aliphatic group, a substituted aliphatic group, an aromatic group or a substituted aromatic group. Y is O—, CH2—, CH2CH2— or CH═CH— and is bonded to a carbon atom in Phenyl Ring A that is ortho to R1. R4-R6 are independently H, an aliphatic group, a substituted aliphatic group, an aromatic group or a substituted aromatic group. n and m are independently 0, 1 or 2.
摘要翻译： 公开了由结构式（I）表示的化合物：Ar是取代或未取代的芳基。 Q是共价键，-CH 2 - 或-CH 2 CH 2 - ; W是长度为2至10个原子，优选2至7个长度的取代或未取代的亚烷基或取代或未取代的亚烷基连接基团。 除了R 1和W之外，苯环A任选被至多四个取代基取代，R 2是（CH 2）n -CH（OR 2） - （CH 2）nE， - （CH）= C（OR 2） - （CH 2） - （CH 2）n -CH（Y） - （CH 2）mE或（CH）= C（Y）（CH 2）mE; 其中E是COOR 3，C 1 -C 3烷基腈，甲酰胺，磺酰胺，酰基磺酰胺或四唑，其中磺酰胺，酰基磺酰胺和四唑任选地被一个或多个独立地选自：C 1 -C 6烷基，卤代烷基和芳基-C 1-4 - ; R 2是H，脂族基团，取代的脂族基团，卤代烷基，芳族基团，取代的芳族基团，-COR 4，-COOR 4，-CONR 5 R 6，-C（S）R 4，-C（S）OR 4或C ）NR 5 R 6，R 3为H，脂族基团，取代的脂族基团，芳族基团或取代的芳族基团。 Y是O-，CH 2 - ，CH 2 CH 2 - 或CH = CH-，并且与R 1邻位的苯基环A中的碳原子键合。 R 4 -R 6独立地为H，脂族基团，取代的脂族基团，芳族基团或取代的芳族基团。 n和m独立地为0,1或2。
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