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1. 发明授权

US06403582B2 Substituted oximes and hydrazones as neurokinin antagonists 失效
标题翻译：取代的肟和腙作为神经激肽拮抗剂
公开(公告)号：US06403582B2
公开(公告)日：2002-06-11
申请号：US09759045
申请日：2001-01-12
申请人： Gregory A. Reichard , Neng-Yang Shih , Dasong Wang
发明人： Gregory A. Reichard , Neng-Yang Shih , Dasong Wang
IPC分类号： C07D23504
CPC分类号： C07D401/04 , C07D401/06 , C07D401/14 , C07D403/06
摘要： Compound represented by the structural formula or a pharmaceutically acceptable salt thereof, wherein: a is 0-3; b, d and e are 0-2; R is H, alkyl, F or —OR6; A is an optionally substituted oxime or hydrazone; d is not 0 and X is a bond, —C(O)—, —O—, —NR9—, —S(O)e—, —N(R6)C(O)—, —C(O)N(R6)—, —OC(O)NR6—, —OC(═S)NR6—, —N(R6)C(═S)O—, —S(O)2N(R6)—, —N(R6)S(O)2—, —N(R6)C(O)O—, —OC(O)— or —N(R6)C(O)NR7—; or d is 0 and X is a bond or —NR6—; T is H, aryl, heterocycloalkyl or heteroaryl; Q is phenyl, naphthyl or heteroaryl; R6 is H, alkyl, hydroxyalkyl, alkoxyalkyl, phenyl, and benzyl; R9 is R6 or —OR6 R6a, R7a, R8a and R9a are H or alkyl; Z is a nitrogen-containing heterocyclo group, e.g., piperidinyl, substituted by a heterocyclo- or heterocycloalkyl group; wherein phenyl, benzyl, aryl, heterocycloalkyl, heteroaryl and cycloalkyl groups are optionally substituted; methods of treating diseases such as asthma, cough, bronchospasm, depression, emesis, imflammatory diseases, and gastrointestinal disorders with said compounds, and pharmaceutical compositions comprising said compounds are disclosed.
摘要翻译：由结构式表示的化合物或其药学上可接受的盐，其中：a为0-3; b，d和e为0-2; R为H，烷基，F或-OR 6; A为任选取代的肟或腙; （O） - ， - O - ， - NR9 - ， - S（O）e - ， - N（R6）C（O） - ， - （O）（R6） - ， - OC（O）NR6-，-OC（= S）NR6-，-N（R6）C（= S）O-，-S（O））S（O）2 - ， - N（R 6）C（O）O-，-OC（O） - 或-N（R 6）C（O）NR 7 - 或者d是0，X是一个键或-NR6-; T是H，芳基，杂环烷基或杂芳基; Q是苯基，萘基或杂芳基; R6是H，烷基，羟基烷基，烷氧基烷基，苯基和苄基; R9是R6 或-OR6R6a，R7a，R8a和R9a是H或烷基; Z是含氮杂环基，例如被杂环基或杂环烷基取代的哌啶基;其中苯基，苄基，芳基，杂环烷基，杂芳基和环烷基是任选取代; 公开了用所述化合物治疗哮喘，咳嗽，支气管痉挛，抑郁症，呕吐，炎性疾病和胃肠道疾病等疾病的方法，以及包含所述化合物的药物组合物。

2. 发明授权

US06204265B1 Substituted oximes and hydrazones as neurokinin antagonists 失效
标题翻译：取代的肟和腙作为神经激肽拮抗剂
公开(公告)号：US06204265B1
公开(公告)日：2001-03-20
申请号：US09468591
申请日：1999-12-21
申请人： Gregory A. Reichard , Neng-Yang Shih , Dasong Wang
发明人： Gregory A. Reichard , Neng-Yang Shih , Dasong Wang
IPC分类号： C07D23904
CPC分类号： C07D401/04 , C07D401/06 , C07D401/14 , C07D403/06
摘要： Compound represented by the structural formula or a pharmaceutically acceptable salt thereof, wherein: a is 0-3; b, d and e are 0-2; R is H, alkyl, F or —OR6; A is an optionally substituted oxime or hydrazone; d is not 0 and X is a bond, —C(O)—, —O—, —NR9—, —S(O)e—, —N(R6)C(O)—, —C(O)N(R6)—, —OC(O)NR6—, —OC(═S)NR6—, —N(R6)C(═S)O—, —S(O)2N(R6)—, —N(R6)S(O)2—, —N(R6)C(O)O—, —OC(O)— or —N(R6)C(O)NR7—; or d is 0 and X is a bond or —NR6—; T is H, aryl, heterocycloalkyl or heteroaryl; Q is phenyl, naphthyl or heteroaryl; R6 is H, alkyl, hydroxyalkyl, alkoxyalkyl, phenyl, and benzyl; R9 is R6 or —OR6 R6a, R7a, R8a and R9a are H or alkyl; Z is a nitrogen-containing heterocyclo group, e.g., piperidinyl, substituted by a heterocyclo- or heterocycloalkyl group; wherein phenyl, benzyl, aryl, heterocycloalkyl, heteroaryl and cycloalkyl groups are optionally substituted; methods of treating diseases such as asthma, cough, bronchospasm, depression, emesis, imflammatory diseases, and gastrointestinal disorders with said compounds, and pharmaceutical compositions comprising said compounds are disclosed.
摘要翻译：由结构式表示的化合物或其药学上可接受的盐，其中：a为0-3; b，d和e为0-2; R为H，烷基，F或-OR 6; A为任选取代的肟或腙; （O） - ， - O - ， - NR9 - ， - S（O）e - ， - N（R6）C（O） - ， - （O）（R6） - ， - OC（O）NR6-，-OC（= S）NR6-，-N（R6）C（= S）O-，-S（O））S（O）2 - ， - N（R 6）C（O）O-，-OC（O） - 或-N（R 6）C（O）NR 7 - 或者d是0，X是一个键或-NR6-; T是H，芳基，杂环烷基或杂芳基; Q是苯基，萘基或杂芳基; R6是H，烷基，羟基烷基，烷氧基烷基，苯基和苄基; R9是R6 或-OR6R6a，R7a，R8a和R9a是H或烷基; Z是含氮杂环基，例如被杂环基或杂环烷基取代的哌啶基;其中苯基，苄基，芳基，杂环烷基，杂芳基和环烷基是任选取代; 公开了用所述化合物治疗哮喘，咳嗽，支气管痉挛，抑郁症，呕吐，炎性疾病和胃肠道疾病等疾病的方法，以及包含所述化合物的药物组合物。

3. 发明授权

US06534502B2 Substituted oximes and hydrazones as neurokinin antagonists 失效
公开(公告)号：US06534502B2
公开(公告)日：2003-03-18
申请号：US10047836
申请日：2001-10-23
申请人： Gregory A. Reichard , Neng-Yang Shih , Dasong Wang
发明人： Gregory A. Reichard , Neng-Yang Shih , Dasong Wang
IPC分类号： C07D23504
CPC分类号： C07D401/04 , C07D401/06 , C07D401/14 , C07D403/06
摘要： Compound represented by the structural formula or a pharmaceutically acceptable salt thereof, wherein: a is 0-3; b, d and e are 0-2; R is H, alkyl, F or —OR6; A is an optionally substituted oxime or hydrazone; d is not 0 and X is a bond, —C(O)—, —O—, —NR9—, —S(O)e—, —N(R6)C(O)—, —C(O)N(R6)—, —OC(O)NR6—, —OC(═S)NR6—, —N(R6)C(═S)O—, —S(O)2N(R6)—, —N(R6)S(O)2—, —N(R6)C(O)O—, —OC(O)— or —N(R6)C(O)NR7—; or d is 0 and X is a bond or —NR6—; T is H, aryl, heterocycloalkyl or heteroaryl; Q is phenyl, naphthyl or heteroaryl; R6 is H, alkyl, hydroxyalkyl, alkoxyalkyl, phenyl, and benzyl; R9 is R6 or —OR6 R6a, R7a, R8a and R9a are H or alkyl; Z is a nitrogen-containing heterocyclo group, e.g., piperidinyl, substituted by a heterocyclo- or heterocycloalkyl group; wherein phenyl, benzyl, aryl, heterocycloalkyl, heteroaryl and cycloalkyl groups are optionally substituted; methods of treating diseases such as asthma, cough, bronchospasm, depression, emesis, imflammatory diseases, and gastrointestinal disorders with said compounds, and pharmaceutical compositions comprising said compounds are disclosed.

4. 发明授权

US08273895B2 NK1 antagonists 有权
标题翻译： NK1拮抗剂
公开(公告)号：US08273895B2
公开(公告)日：2012-09-25
申请号：US12967132
申请日：2010-12-14
申请人： Sunil Paliwal , Gregory A. Reichard , Cheng Wang , Dong Xiao , Hon-Chung Tsui , Neng-Yang Shih , Juan D. Arredondo , Michelle Laci Wrobleski , Anandan Palani
发明人： Sunil Paliwal , Gregory A. Reichard , Cheng Wang , Dong Xiao , Hon-Chung Tsui , Neng-Yang Shih , Juan D. Arredondo , Michelle Laci Wrobleski , Anandan Palani
IPC分类号： C07D211/20 , C07D207/12 , A61K31/45 , A61K31/451
CPC分类号： C07D498/10 , A61K31/166 , A61K31/40 , A61K31/4025 , A61K31/437 , A61K31/4375 , A61K31/438 , A61K31/451 , A61K31/454 , A61K31/4545 , A61K31/537 , A61K31/5377 , A61K31/573 , A61K45/06 , C07D207/14 , C07D207/50 , C07D211/28 , C07D211/32 , C07D211/42 , C07D211/56 , C07D211/60 , C07D211/72 , C07D211/76 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D413/10 , C07D413/12 , C07D471/10 , C07D487/10 , C07D491/10 , C07D513/10
摘要： A NK1 antagonist having the formula (I), wherein Ar1 and Ar2 are optionally substituted phenyl or heteroaryl, X1 is an ether, thio or imino linkage, R4 and R5 are not both H or alkyl, and the remaining variables are as defined in the specification, useful for treating a number of disorders, including emesis, depression, anxiety and cough. Pharmaceutical compositions. Methods of treatment and combinations with other agents are also disclosed.
摘要翻译：具有式（I）的NK1拮抗剂，其中Ar1和Ar2是任选取代的苯基或杂芳基，X1是醚，硫代或亚氨基键，R4和R5不都是H或烷基，其余的变量如规范，用于治疗许多疾病，包括呕吐，抑郁，焦虑和咳嗽。药物组合物。还公开了治疗方法和与其它药剂的组合。

5. 发明授权

US06635630B2 Selective neurokinin antagonists 失效
标题翻译：选择性神经激肽拮抗剂
公开(公告)号：US06635630B2
公开(公告)日：2003-10-21
申请号：US10163663
申请日：2002-06-06
申请人： Neng-Yang Shih , Ho-Jane Shue , Gregory A. Reichard , Sunil Paliwal , David J. Blythin , John J. Piwinski , Dong Xiao , Xiao Chen
发明人： Neng-Yang Shih , Ho-Jane Shue , Gregory A. Reichard , Sunil Paliwal , David J. Blythin , John J. Piwinski , Dong Xiao , Xiao Chen
IPC分类号： A61K31330
CPC分类号： C07D239/10 , C07C45/71 , C07C217/48 , C07D211/58 , C07D233/14 , C07D233/16 , C07D233/22 , C07D233/30 , C07D233/32 , C07D233/42 , C07D233/46 , C07D233/48 , C07D233/78 , C07D285/10 , C07D401/04 , C07D401/12 , C07D403/12 , C07D409/06 , C07D413/04 , C07D413/06 , C07D413/10 , C07F9/6506 , C07C47/575
摘要： Compound represented by the structural formula or a pharmaceutically acceptable salt thereof, wherein Ar1 and Ar2 are optionally substituted heteroaryl or optionally substituted phenyl; X1 is —O—, —S—, —SO—, —SO2—, —NR12—, —NCOR12— or —NR12SO2R15; is selected from the group consisting of X2 is —O—, —S— or —NR5—; Y is ═O, ═S or ═NR11; Y1 is H, C1-C6 alkyl, —NR17R13, —SCH3, R19-aryl(CH2)n6—, R19-heteroaryl-(CH2)n6—, —(CH2)n6—heterocycloalkyl, —(C1-C3)alkyl-NH—C(O)O(C1-C6)alkyl or —NHC(O)R15; R5 is H or —(CH2)n1—G, wherein n1 is 0-5, G is H, —CF3, —CHF2, —CH2F, —OH, —O—(C1-C6 alkyl), —SO2R13, —O—(C3-C8 cycloalkyl), —NR13R14, —SO2NR13R14, —NR13SO2R15, —NR13COR12, —NR12(CONR13R14), —CONR13R14, —COOR12, C3-C8 cycloalkyl, R19-aryl, R19-heteroaryl, and provided when n1=0, G is not H; R1, R2, R3 and R7 are H, alkyl, cycloalkyl, —CHF2, —CH2F or —CF3; or R1 and R2, together with the carbon to which they are attached, form an alkylene ring; or R1 and R2 together are ═O; R6 is R7 or —OH; and the remaining variables are as defined in the specification, methods of treating diseases susceptible to treatment with neurokinin antagonists with said compounds, and pharmaceutical compositions comprising said compounds are disclosed. Also disclosed are pharmaceutical compositions comprising an effective amount of a compound of claim 1, at least one pharmaceutically acceptable carrier, and in combination with an effective amount of a selective serotonin reuptake inhibitor.
摘要翻译：由结构式表示的化合物或其药学上可接受的盐，其中Ar 1和Ar 2是任选取代的杂芳基或任选取代的苯基; X 1是-O - ， - S - ， - SO-，-SO 2 - ，-NR 12 - ， - NR C 12 - 或-NR 12 SO 2 R 15选自X 2是-O - ， - S-或-NR 5 - ; Y是= O，= S或= NR 11; Y 1是H，C 1 -C 6烷基，-NR 17 R 13，-SCH 3，R 19 - 芳基（CH 2）n6 - （CH 2）n6 - ， - （CH 2）n 6-杂环烷基， - （C 1 -C 3）烷基-NH-C（O）O（C 1 -C 6）烷基或-NHC（O） R 15; R 5是H或 - （CH 2）n1-G，其中n1是0-5，G是H，-CF 3，-CHF 2，-CH 2 F，-OH，-O-（C 1 -C 6 烷基），-SO 2 R 13，-O-（C 3 -C 8环烷基），-NR 13 R 14，-SO 2 NR 13 R 14，-NR 13 SO 2 R 15， NR 13 R 12，-NR 12（CONR 13 R 14），-CONR 13 R 14，-COOR 12，C 3 -C 8环烷基，R 19 芳基，R 19 - 杂芳基，并且当n 1 = 0时，G不为H; R 1，R 2，R 3和R 7为H，烷基，环烷基，-CHF 2 ，-CH2F或-CF3; 或R 1和R 2与它们所连接的碳一起形成亚烷基环; 或R 1和R 2一起为= O; R 6为R 7或-OH;其余变量如本说明书中所定义，治疗易受神经激肽拮抗剂治疗的疾病的方法，所述化合物和包含所述化合物的药物组合物。还公开了药物组合物，其包含有效量的权利要求1的化合物，至少一种药学上可接受的载体，并与有效量的选择性5-羟色胺再摄取抑制剂组合。

6. 发明授权

US06436928B1 Selective neurokinin antagonists 失效
标题翻译：选择性神经激肽拮抗剂
公开(公告)号：US06436928B1
公开(公告)日：2002-08-20
申请号：US09737036
申请日：2000-12-14
申请人： Neng-Yang Shih , Ho-Jane Shue , Gregory A. Reichard , Sunil Paliwal , David J. Blythin , John J. Piwinski , Dong Xiao , Xiao Chen
发明人： Neng-Yang Shih , Ho-Jane Shue , Gregory A. Reichard , Sunil Paliwal , David J. Blythin , John J. Piwinski , Dong Xiao , Xiao Chen
IPC分类号： A61K314166
CPC分类号： C07D239/10 , C07C45/71 , C07C217/48 , C07D211/58 , C07D233/14 , C07D233/16 , C07D233/22 , C07D233/30 , C07D233/32 , C07D233/42 , C07D233/46 , C07D233/48 , C07D233/78 , C07D285/10 , C07D401/04 , C07D401/12 , C07D403/12 , C07D409/06 , C07D413/04 , C07D413/06 , C07D413/10 , C07F9/6506 , C07C47/575
摘要： A compound represented by the structural formula or a pharmaceutically acceptable salt thereof, wherein Ar1 and Ar2 are optionally substituted heteroaryl or optionally substituted phenyl; X1 is —O—, —SO0-2—, —NR12—, —NCOR12— or —NR12SO2R15; is X2 is —O—, —S— or optionally substituted nitrogen; Y is ═O, ═S or ═NR11; Y1 is H, alkyl, —NR17R13, —SCH3, R19-aryl(CH2)n6—, R19-heteroaryl-(CH2)n6—, —(CH2)n6-heterocycloalkyl, -alkyl-NH—C(O)O-alkyl or —NHC(O)R15; R1, R2, R3 and R7 are H, alkyl, OH-alkyl, cycloalkyl, —CHF2, —CH2F or —CF3; or R1 and R2 form an alkylene ring; or R1 and R2 together are ═O; R6 is H, alkyl, —OR13 or —SR12; and the remaining variables are as defined in the specification, is disclosed, as well as a pharmaceutical compositions comprising said compound, methods of using said compound as a neurokinin antagonist, and the combination of said compounds with a selective serotonin reuptake inhibitor.
摘要翻译：由结构式表示的化合物或其药学上可接受的盐，其中Ar 1和Ar 2是任选取代的杂芳基或任选取代的苯基; X 1是-O-，-SOO 2 - ， - NR 12 - ， - NRCOR 12 - 或-NR 12 SO 2 R 15; isX2是-O - ， - S-或任选取代的氮; Y是= O，= S或= NR 11; Y 1是H，烷基，-NR 17 R 13，-SCH 3，R 19 - 芳基（CH 2）n6 - ，R 19 - （CH2）n6-， - （CH2）n6-杂环烷基， - 烷基-NH-C（O）O-烷基或-NHC（O）R15; R1，R2，R3和R7是H，烷基，环烷基，-CHF 2，-CH 2 F或-CF 3; 或R 1和R 2形成亚烷基环; 或R 1和R 2一起为= O; R 6为H，烷基，-OR 13或-SR 12;其余变量如本说明书中所定义，以及包含所述化合物的药物组合物，使用所述化合物的方法作为神经激肽拮抗剂，以及所述化合物与选择性5-羟色胺再摄取抑制剂的组合。

7. 发明授权

US6063926A Substituted oximes as neurokinin antagonists 失效
标题翻译：取代肟作为神经激肽拮抗剂
公开(公告)号：US6063926A
公开(公告)日：2000-05-16
申请号：US195429
申请日：1998-11-18
申请人： Gregory A. Reichard , Cheryl A. Alaimo , Neng-Yang Shih , Pauline C. Ting , Nicholas I. Carruthers , Brian J. Lavey
发明人： Gregory A. Reichard , Cheryl A. Alaimo , Neng-Yang Shih , Pauline C. Ting , Nicholas I. Carruthers , Brian J. Lavey
IPC分类号： C07D211/24 , C07D211/52 , C07D211/58 , C07D211/62 , C07D211/76 , C07D211/94 , C07D401/12 , C07D401/14 , C07D417/14 , C07D401/00 , C07D211/26 , C07D211/44 , C07D211/68
CPC分类号： C07D401/12 , C07D211/24 , C07D211/52 , C07D211/58 , C07D211/62 , C07D211/76 , C07D211/94 , C07D401/14 , C07D417/14
摘要： Compounds within the genus represented by the structural formula I ##STR1## or a pharmaceutically acceptable salt thereof, wherein: T is substituted phenyl or substituted pyridyl; ##STR2## R.sup.4 is methyl or ethyl; and Z is substituted piperidinyl.
摘要翻译：由结构式I表示的属的化合物或其药学上可接受的盐，其中：T是取代的苯基或取代的吡啶基; R4是甲基或乙基; Z是取代的哌啶基。

8. 发明授权

US07902366B2 NK1 antagonists 有权
标题翻译： NK1拮抗剂
公开(公告)号：US07902366B2
公开(公告)日：2011-03-08
申请号：US11358827
申请日：2006-02-21
申请人： Sunil Paliwal , Gregory A. Reichard , Cheng Wang , Dong Xiao , Hon-Chung Tsui , Neng-Yang Shih , Juan D. Arredondo , Michelle Laci Wrobleski , Anandan Palani
发明人： Sunil Paliwal , Gregory A. Reichard , Cheng Wang , Dong Xiao , Hon-Chung Tsui , Neng-Yang Shih , Juan D. Arredondo , Michelle Laci Wrobleski , Anandan Palani
IPC分类号： A61K31/445 , C07D211/12
CPC分类号： C07D498/10 , A61K31/166 , A61K31/40 , A61K31/4025 , A61K31/437 , A61K31/4375 , A61K31/438 , A61K31/451 , A61K31/454 , A61K31/4545 , A61K31/537 , A61K31/5377 , A61K31/573 , A61K45/06 , C07D207/14 , C07D207/50 , C07D211/28 , C07D211/32 , C07D211/42 , C07D211/56 , C07D211/60 , C07D211/72 , C07D211/76 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D413/10 , C07D413/12 , C07D471/10 , C07D487/10 , C07D491/10 , C07D513/10
摘要： A NK1 antagonist having the formula (I), wherein Ar1 and Ar2 are optionally substituted phenyl or heteroaryl, X1 is an ether, thio or imino linkage, R4 and R5 are not both H or alkyl, and the remaining variables are as defined in the specification, useful for treating a number of disorders, including emesis, depression, anxiety and cough. Pharmaceutical compositions. Methods of treatment and combinations with other agents are also disclosed.
摘要翻译：具有式（I）的NK1拮抗剂，其中Ar1和Ar2是任选取代的苯基或杂芳基，X1是醚，硫代或亚氨基键，R4和R5不都是H或烷基，其余的变量如规范，用于治疗许多疾病，包括呕吐，抑郁，焦虑和咳嗽。药物组合物。还公开了治疗方法和与其它药剂的组合。

9. 发明授权

US5696267A Substituted oximes, hydrazones and olefins as neurokinin antagonists 失效
标题翻译：取代的肟，腙和烯烃作为神经激肽拮抗剂
公开(公告)号：US5696267A
公开(公告)日：1997-12-09
申请号：US641384
申请日：1996-04-30
申请人： Gregory A. Reichard , Robert G. Aslanian , Cheryl A. Alaimo , Michael P. Kirkup , Andrew Lupo, Jr. , Pietro Mangiaracina , Kevin D. McCormick , John J. Piwinski , Bandarpalle B. Shankar , Neng-Yang Shih , James M. Spitler , Pauline C. Ting , Ashit Ganguly , Nicholas I. Carruthers
发明人： Gregory A. Reichard , Robert G. Aslanian , Cheryl A. Alaimo , Michael P. Kirkup , Andrew Lupo, Jr. , Pietro Mangiaracina , Kevin D. McCormick , John J. Piwinski , Bandarpalle B. Shankar , Neng-Yang Shih , James M. Spitler , Pauline C. Ting , Ashit Ganguly , Nicholas I. Carruthers
IPC分类号： C07D295/12 , A61K31/397 , A61K31/40 , A61K31/415 , A61K31/4178 , A61K31/439 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/4436 , A61K31/445 , A61K31/4465 , A61K31/4468 , A61K31/45 , A61K31/451 , A61K31/452 , A61K31/4523 , A61K31/4525 , A61K31/454 , A61K31/4545 , A61K31/47 , A61K31/4709 , A61K31/495 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/505 , A61K31/506 , A61K31/535 , A61K31/5375 , A61K31/5377 , A61P1/00 , A61P11/00 , A61P25/00 , A61P29/00 , A61P43/00 , C07D205/04 , C07D207/08 , C07D207/12 , C07D207/14 , C07D211/52 , C07D211/58 , C07D211/76 , C07D295/13 , C07D295/185 , C07D333/22 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D405/12 , C07D409/06 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/12 , C07D451/04 , C07D211/08
CPC分类号： C07D295/185 , C07D211/52 , C07D211/58 , C07D211/76 , C07D295/13 , C07D333/22 , C07D401/04 , C07D401/06 , C07D409/06 , C07D413/12 , C07D413/14 , C07D417/12
摘要： Compound represented by the structural formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein: a is 0, 1, 2 or 3;b, d and e are independently 0, 1 or 2; R is H, C.sub.1-6 alkyl, --OH or C.sub.2 -C.sub.6 hydroxyalkyl; A is an optionally substituted oxime, hydrazone or olefin; X is a bond, --C(O)--, --O--, --NR.sup.6 --, --S(O).sub.e --, --N(R.sup.6)C(O)--, --C(O)N(R.sup.6)--OC(O)NR.sup.6 --, --OC(.dbd.S)NR.sup.6 --, --N(R.sup.6)C(.dbd.S)O--, --C(.dbd.NOR.sup.1)--, --S(O).sub.2 N(R.sup.6)--, --N(R.sup.6)S(O).sub.2 --,--N(R.sup.6)C(O)O-- or --OC(O)--; T is H, phthalimidyl, aryl, heterocycloalkyl, heteroaryl, cycloalkyl or bridged cycloalkyl; Q is --SR.sup.6, --N(R.sup.6)(R.sup.7), --OR.sup.6, phenyl, naphthyl or heteroaryl; R.sup.6a, R.sup.7a, R.sup.8a, R.sup.9a, R.sup.6 and R.sup.7 are H, C.sub.1-6 alkyl, C.sub.2 -C.sub.6 hydroxyalkyl, C.sub.1 -C.sub.6 alkoxy-C.sub.1 -C.sub.6 alkyl, phenyl or benzyl; or R.sup.6 and R.sup.7, together with the nitrogen to which they are attached, form a ring; R.sup.9a is R.sup.6 or --OR.sup.6 ; Z is morpholinyl, optionally N-substituted piperazinyl, optionally substituted ##STR2## or substituted ##STR3## g is 0-3 and h is 1-4, provided the sum of h and g is 1-7; wherein aryl, heterocycloalkyl, heteroaryl, cycloalkyl and bridged cycloalkyl groups are optionally substituted; methods of treating asthma, cough, bronchospasm, imflammatory diseases, and gastrointestinal disorders with said compounds, and pharmaceutical compositions comprising said compounds are disclosed.
摘要翻译：由结构式I表示的化合物或其药学上可接受的盐，其中：a为0,1,2或3; b，d和e独立地为0,1或2; R为H，C 1-6烷基，-OH或C 2 -C 6羟基烷基; A是任选取代的肟，腙或烯烃; X是键，-C（O） - ， - O - ， - NR6 - ， - S（O）e - ， - N（R6）C（O） - ， - （O）NR6-， - OC（= S）NR6-，-N（R6）C（= S）O-，-C（= NOR1） - ， - S（O） R6）S（O）2 - ， - N（R6）C（O）O-或-OC（O） - ; T是H，苯偶酰亚氨基，芳基，杂环烷基，杂芳基，环烷基或桥连环烷基; Q是-SR 6，-N（R 6）（R 7），-OR 6，苯基，萘基或杂芳基; R6a，R7a，R8a，R9a，R6和R7是H，C1-6烷基，C2-C6羟基烷基，C1-C6烷氧基-C1-C6烷基，苯基或苄基; 或R 6和R 7与它们所连接的氮一起形成环; R9a为R6或-OR6; Z是吗啉基，任选取代的哌嗪基，任选取代的取代的或取代的，如果h和g之和为1-7，则g是0-3，h是1-4; 其中芳基，杂环烷基，杂芳基，环烷基和桥连环烷基任选被取代; 公开了用所述化合物治疗哮喘，咳嗽，支气管痉挛，炎性疾病和胃肠道疾病的方法，以及包含所述化合物的药物组合物。

10. 发明授权

US07049320B2 NK1 antagonists 有权
公开(公告)号：US07049320B2
公开(公告)日：2006-05-23
申请号：US10321687
申请日：2002-12-17
申请人： Sunil Paliwal , Gregory A. Reichard , Cheng Wang , Dong Xiao , Hon-Chung Tsui , Neng-Yang Shih , Juan D. Arredondo , Michelle Laci Wrobleski , Anandan Palani
发明人： Sunil Paliwal , Gregory A. Reichard , Cheng Wang , Dong Xiao , Hon-Chung Tsui , Neng-Yang Shih , Juan D. Arredondo , Michelle Laci Wrobleski , Anandan Palani
IPC分类号： A61K31/44 , C07D221/20
CPC分类号： C07D498/10 , A61K31/166 , A61K31/40 , A61K31/4025 , A61K31/437 , A61K31/4375 , A61K31/438 , A61K31/451 , A61K31/454 , A61K31/4545 , A61K31/537 , A61K31/5377 , A61K31/573 , A61K45/06 , C07D207/14 , C07D207/50 , C07D211/28 , C07D211/32 , C07D211/42 , C07D211/56 , C07D211/60 , C07D211/72 , C07D211/76 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D413/10 , C07D413/12 , C07D471/10 , C07D487/10 , C07D491/10 , C07D513/10
摘要： A NK1 antagonist having the formula (I), wherein Ar1 and Ar2 are optionally substituted phenyl or heteroaryl, X1 is an ether, thio or imino linkage, R4 and R5 are not both H or alkyl, and the remaining variables are as defined in the specification, useful for treating a number of disorders, including emesis, depression, anxiety and cough. Pharmaceutical compositions. Methods of treatment and combinations with other agents are also disclosed.

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