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1. 发明申请

WO2003082861A3 MORPHOLINYL-UREA DERIVATIVES FOR USE OF THE TREATMENT OF INFLAMMATORY DISEASES 审中-公开
公开(公告)号：WO2003082861A3
公开(公告)日：2003-10-09
申请号：PCT/EP2003/003335
申请日：2003-03-27
申请人： GLAXO GROUP LIMITED , ANCLIFF, Rachael, Ann , COOK, Caroline, Mary , ELDRED, Colin, David , GORE, Paul, Martin , HARRISON, Lee, Andrew , HAYES, Martin, Alistair , HODGSON, Simon, Teanby , JUDD, Duncan, Bruce , KEELING, Suzanne, Elaine , LEWELL, Xiao, Qing , MILLS, Gail , ROBERTSON, Graeme, Michael , SWANSON, Stephen , WALKER, Andrew, John , WILKINSON, Mark
发明人： ANCLIFF, Rachael, Ann , COOK, Caroline, Mary , ELDRED, Colin, David , GORE, Paul, Martin , HARRISON, Lee, Andrew , HAYES, Martin, Alistair , HODGSON, Simon, Teanby , JUDD, Duncan, Bruce , KEELING, Suzanne, Elaine , LEWELL, Xiao, Qing , MILLS, Gail , ROBERTSON, Graeme, Michael , SWANSON, Stephen , WALKER, Andrew, John , WILKINSON, Mark
IPC分类号： C07D413/12
摘要： Compounds of formula (I) wherein: R1 represents substituted or unsubstituted heteroaryl; Y represents -(CRnaRnb)n-; Rna and Rnb are each independently hydrogen or C1-6alkyl; n is an integer from 0 to 5;R2 represents unsubstituted or substituted aryl or unsubstituted or substituted heteroaryl; R3 and R4 each independently represent hydrogen or C1-6alkyl; R7 represents hydrogen or C1-6alkyl; R8 represents hydrogen or C1-6alkyl;and salts and solvates thereof;are CCR3 antagonists and are thus indicated to be useful in therapy.

2. 发明申请

WO2003082835A1 PROCESS FOR THE PREPARATION OF MORPHOLINE DERIVATIVES AND INTERMEDIATES THEREFORE 审中-公开
标题翻译：因此，制备摩尔衍生物及其中间体的方法
公开(公告)号：WO2003082835A1
公开(公告)日：2003-10-09
申请号：PCT/EP2003/003343
申请日：2003-03-27
申请人： GLAXO GROUP LIMITED , HAYES, Martin, Alistair , MILLS, Gail , SWANSON, Stephen , WALKER, Andrew, John , WILKINSON, Mark
发明人： HAYES, Martin, Alistair , MILLS, Gail , SWANSON, Stephen , WALKER, Andrew, John , WILKINSON, Mark
IPC分类号： C07D265/30
CPC分类号： C07D209/48 , C07D265/30 , C07D413/06
摘要： Processes for the preparation of a compound of formula (IIIA)(I), or a salt thereof; wherein; Z represents a bond, CO, SO 2 , CR 10 R 7 (CH 2 ) n , (CH 2 ) n CR 10 R 7 , CHR 7 (CH 2 )n O , CHR 7 (CH 2 ) n S, CHR 7 (CH 2 ) n OCO, CHR 7 (CH 2 ) n CO, COCHR 7 (CH 2 ) n or SO 2 CHR 7 (CH 2 ) n ; R 6 represents C 1-6 alkyl, C 2-6 alkenyl, aryl, heteroaryl, aryl-C 2-6 alkenyl-, -CN or a group of formula -Y 2 -J 3 ; R 7 represents hydrogen, C 1-4 alkyl, CONR 8 R 9 or COOC 1-6 alkyl;a and b represent 1 or 2, such that a+b represents 2 or 3;n represents an integer from 0 to 4; M represents a C 3-8 cycloalkyl or C 3-8 cycloalkenyl group fused to a monocyclic aryl or monocyclic heteroaryl group; J 3 represents a moiety of formula (K): (II), wherein X 1 represents oxygen, NR 11 or sulphur, X 2 represents CH 2 , oxygen, NR 12 or sulphur, m 1 represents an integer from 1 to 3 and m 2 represents an integer from 1 to 3, provided that m 1 +m 2 is in the range from 3 to 5, also provided that when both X 1 and X 2 represent oxygen, NR 11 , NR 12 or sulphur, m 1 and m 2 must both not equal less than 2, wherein (K) is optionally substituted by one or more (eg. 1 or 2) -Y 3 -aryl, -Y 3 -heteroaryl, -Y 3 -CO-aryl, -COC 3-8 cycloalkyl, -Y 3 -CO-heteroaryl, -C 1-6 alkyl, -Y 3 -COOC 1-6 alkyl, -Y 3 -COC 1-6 alkyl, -Y 3 -W, -Y 3 -CO-W, -Y 3 -NR 15 R 16 , -Y 3 -CONR 15 R 16 , hydroxy, oxo, -Y 3 -SO 2 NR 15 R 16 , -Y 3 -SO 2 C 1-6 alkyl, -Y 3 -SO 2 aryl, -Y 3 -SO 2 heteroaryl, -Y 3 -NR 13 C 1-6 alkyl, -Y 3 -NR 13 SO 2 C 1-6 alkyl, -Y 3 -NR 13 CONR 15 R 16 , -Y 3 -NR 13 COOR 14 or -Y 3 -OCONR 15 R 16 groups, and is optionally fused to a monocyclic aryl or heteroaryl ring; R 8 , R 9 , R 10 , R 11 , R 12 , R 13 and R 14 independently represent hydrogen or C 1-6 alkyl; R 15 and R 16 independently represent hydrogen or C 1-6 alkyl or R 15 and R 16 together with the nitrogen atom to which they are attached may form a morpholine, piperidine or pyrrolidine ring; R 17 and R 18 independently represent hydrogen or C 1-6 alkyl; W represents a saturated or unsaturated, non-aromatic 5-7 membered ring containing between 1 and 3 heteroatoms selected from nitrogen, oxygen or sulphur, optionally substituted with one or more C 1-6 alkyl, halogen or hydroxy groups; Y 1 , Y 2 and Y 3 independently represent a bond or a group of formula -(CH 2 ) p CR c R d (CH 2 ) q - wherein R c and R d independently represent hydrogen or C 1-4 alkyl or R c and R d may together with the carbon atom to which they are attached form a C 3-8 cycloalkyl group, and p and q independently represent an integer from 0 to 5 wherein p + q is an integer from 0 to 5;, and; k is 1 or 2;are disclosed.
摘要翻译：制备式（IIIA）（I）化合物或其盐的方法; 其中; Z表示键，CO，SO 2，CR 10 R 7（CH 2）n，（CH 2）n CR 10 R 7，CHR 7（CH 2）n O，CHR 7，（CH 2）n S，CHR 7（CH 2）nOCO，CHR 7（CH 2）n CO，COCHR 7（CH 2）n或SO 2 CHR 7（CH 2）n; R 6表示C 1-6烷基，C 2-6烯基，芳基，杂芳基，芳基-C 2-6烯基，-CN或式-Y 2 -J 3基团。 R 7表示氢，C 1-4烷基，CONR 8 R 9或COOC 1-6烷基; a和b表示1或2，使得a + b表示2或3; n表示0的整数到4; M表示与单环芳基或单环杂芳基稠合的C3-8环烷基或C3-8环烯基; J 3代表式（K）的部分：（II），其中X 1表示氧，NR 11或硫，X 2表示CH 2，氧，NR 12或硫， 1>表示1〜3的整数，m 2表示1〜3的整数，条件是m 1 + m 2在3〜5的范围内，也可以在X <1 >和X 2代表氧，NR 11，NR 12或硫，m 1和m 2必须都不小于2，其中（K）任选地被一个或多个（例如1或2）-Y 3芳基，-Y 3 - 杂芳基，-Y 3 -CO-芳基，-COC 3 - 8环烷基，-Y 3 -CO-杂芳基，-C 1 -6烷基，-Y 3 -COOC 1-6烷基，-Y 3 -COC 1-6烷基，-Y 3 -W，-Y 3 -CO-W，-Y 3 - NR 15 R 16，-Y 3 -CONR 15 R 16，羟基，氧代，-Y 3 -SO 2 NR 15 R 16，-Y 3 -SO 2 Cl -6烷基，-Y 3 -SO 2芳基，-Y 3 -SO 2杂芳基，-Y 3 -NR 13 C 1-6烷基，-Y 3 -NR 13 SO 2 C 1-6烷基， -Y 3 -NR 13 CONR 15 R 16，-Y 3 -NR 13 COOR 14或-Y 3 -CONR 15 R 16基团，并且任选地与单环芳基或杂芳基环稠合; R 8，R 9，R 10，R 11，R 12，R 13和R 14独立地表示氢或C 1-6烷基; R 15和R 16独立地表示氢或C 1-6烷基或R 15和R 16与它们所连接的氮原子一起形成吗啉，哌啶或吡咯烷环; R 17和R 18独立地表示氢或C 1-6烷基; W表示含有1至3个选自氮，氧或硫的杂原子的饱和或不饱和的非芳族5-7元环，任选被一个或多个C 1-6烷基，卤素或羟基取代; Y 1，Y 2和Y 3独立地表示键或基团 - （CH 2

3. 发明申请

WO2003082295A1 MORPHOLINE DERIVATIVES SUBSTITUTED AT THE 2-POSITION BY A HETEROCYCLYLALKYLUREA GROUP FOR USE AS CCR-3 ANTAGONISTS IN THE TREATMENT OF INFLAMMATORY CONDITIONS 审中-公开
标题翻译：通过在治疗炎症条件下作为CCR-3拮抗剂使用的间苯二酚基团在2位置取代的吗啉衍生物
公开(公告)号：WO2003082295A1
公开(公告)日：2003-10-09
申请号：PCT/EP2003/003349
申请日：2003-03-27
申请人： GLAXO GROUP LIMITED , ANCLIFF, Rachael, Ann , COOK, Caroline, Mary , ELDRED, Colin, David , GORE, Paul, Martin , HARRISON, Lee, Andrew , HAYES, Martin, Alistair , HODGSON, Simon, Teanby , JUDD, Duncan, Bruce , KEELING, Suzanne, Elaine , LEWELL, Xiao, Qing , MILLS, Gail , ROBERTSON, Graeme, Michael , SWANSON, Stephen , WALKER, Andrew, John , WILKINSON, Mark
发明人： ANCLIFF, Rachael, Ann , COOK, Caroline, Mary , ELDRED, Colin, David , GORE, Paul, Martin , HARRISON, Lee, Andrew , HAYES, Martin, Alistair , HODGSON, Simon, Teanby , JUDD, Duncan, Bruce , KEELING, Suzanne, Elaine , LEWELL, Xiao, Qing , MILLS, Gail , ROBERTSON, Graeme, Michael , SWANSON, Stephen , WALKER, Andrew, John , WILKINSON, Mark
IPC分类号： A61K31/5377
CPC分类号： C07D265/30 , C07D413/12
摘要： Certain compounds of formula (I): wherein: R 1 represents substituted or unsubstituted heterocyciyl; Y represents -(CR na R nb ) n -; R na and R nb are each independently hydrogen or C 1-6 alkyl; n is an integer from 1 to 5; R 2 represents unsubstituted or substituted aryl or unsubstituted or substituted, heteroaryl; R 3 and R 4 each independently represent hydrogen or C 1-6 alkyl; and salts and solvates thereof are CCR-3. antagonists and thus are indicated to be useful in therapy of inflammatory conditions.
摘要翻译：某些式（I）化合物：其中：R 1表示取代或未取代的杂环基; Y表示 - （CRnaRnb）n-; Rna和Rnb各自独立地为氢或C 1-6烷基; n为1〜5的整数; R 2表示未取代或取代的芳基或未取代或取代的杂芳基; R 3和R 4各自独立地表示氢或C 1-6烷基; 其盐和溶剂合物是CCR-3。拮抗剂，因此被认为可用于治疗炎性病症。

4. 发明申请

WO2003082292A1 MORPHOLINE DERIVATIVES SUBSTITUTED AT THE 2-POSITION BY AN ARYLALKYLUREA GROUP FOR USE AS CCR-3 ANTAGONISTS IN THE TREATMENT OF INFLAMMATORY CONDITIONS 审中-公开
标题翻译：通过ARYLALKYLUREA集团在2位置取代的多环芳烃衍生物用作治疗炎症条件下的CCR-3拮抗剂
公开(公告)号：WO2003082292A1
公开(公告)日：2003-10-09
申请号：PCT/EP2003/003340
申请日：2003-03-27
申请人： GLAXO GROUP LIMITED , ANCLIFF, Rachael, Ann , COOK, Caroline, Mary , ELDRED, Colin, David , GORE, Paul, Martin , HARRISON, Lee, Andrew , HAYES, Martin, Alistair , HODGSON, Simon, Teanby , JUDD, Duncan, Bruce , KEELING, Suzanne, Elaine , LEWELL, Xiao, Qing , MILLS, Gail , ROBERTSON, Graeme, Michael , SWANSON, Stephen , WALKER, Andrew, John , WILKINSON, Mark
发明人： ANCLIFF, Rachael, Ann , COOK, Caroline, Mary , ELDRED, Colin, David , GORE, Paul, Martin , HARRISON, Lee, Andrew , HAYES, Martin, Alistair , HODGSON, Simon, Teanby , JUDD, Duncan, Bruce , KEELING, Suzanne, Elaine , LEWELL, Xiao, Qing , MILLS, Gail , ROBERTSON, Graeme, Michael , SWANSON, Stephen , WALKER, Andrew, John , WILKINSON, Mark
IPC分类号： A61K31/5377
CPC分类号： C07D265/30 , C07D413/12
摘要： Certain compounds of formula (I); wherein R 1 represents unsubstituted or substituted aryl; Y represents -(CR na R nb ) n -; R na and R nb are each independently hydrogen or C1-6 alkyl; n is an integer from 1 to 5; R 2 represents unsubstituted or substituted aryl or unsubstituted or substituted heteroaryl; R 3 and R 4 each independently represent hydrogen or C 1-6 alkyl; and salts and solvates thereof are CCR3-antagonists and are thus indicated to be useful in therapy of inflammatory conditions.
摘要翻译：某些式（I）化合物; 其中R 1表示未取代或取代的芳基; Y表示 - （CRnaRnb）n-; Rna和Rnb各自独立地为氢或C 1-6烷基; n为1〜5的整数; R 2表示未取代或取代的芳基或未取代或取代的杂芳基; R 3和R 4各自独立地表示氢或C 1-6烷基; 其盐和溶剂化物是CCR3-拮抗剂，因此被认为可用于治疗炎性病症。

5. 发明申请

WO2003082861A2 NOVEL COMPOUNDS 审中-公开
标题翻译：新型化合物
公开(公告)号：WO2003082861A2
公开(公告)日：2003-10-09
申请号：PCT/EP2003/003335
申请日：2003-03-27
申请人： GLAXO GROUP LIMITED , ANCLIFF, Rachael, Ann , COOK, Caroline, Mary , ELDRED, Colin, David , GORE, Paul, Martin , HARRISON, Lee, Andrew , HAYES, Martin, Alistair , HODGSON, Simon, Teanby , JUDD, Duncan, Bruce , KEELING, Suzanne, Elaine , LEWELL, Xiao, Qing , MILLS, Gail , ROBERTSON, Graeme, Michael , SWANSON, Stephen , WALKER, Andrew, John , WILKINSON, Mark
发明人： ANCLIFF, Rachael, Ann , COOK, Caroline, Mary , ELDRED, Colin, David , GORE, Paul, Martin , HARRISON, Lee, Andrew , HAYES, Martin, Alistair , HODGSON, Simon, Teanby , JUDD, Duncan, Bruce , KEELING, Suzanne, Elaine , LEWELL, Xiao, Qing , MILLS, Gail , ROBERTSON, Graeme, Michael , SWANSON, Stephen , WALKER, Andrew, John , WILKINSON, Mark
IPC分类号： C07D413/12
CPC分类号： C07D413/12 , C07D413/14 , C07D417/12
摘要： Compounds of formula (I) wherein: R1 represents substituted or unsubstituted heteroaryl; Y represents -(CRnaRnb)n-; Rna and Rnb are each independently hydrogen or C1-6alkyl; n is an integer from 0 to 5;R2 represents unsubstituted or substituted aryl or unsubstituted or substituted heteroaryl; R3 and R4 each independently represent hydrogen or C1-6alkyl; R7 represents hydrogen or C1-6alkyl; R8 represents hydrogen or C1-6alkyl;and salts and solvates thereof;are CCR3 antagonists and are thus indicated to be useful in therapy.
摘要翻译：式（I）化合物，其中：R 1表示取代或未取代的杂芳基; Y表示 - （CRnaRnb）n-; Rna和Rnb各自独立地为氢或C 1-6烷基; n为0至5的整数; R 2表示未取代或取代的芳基或未取代或取代的杂芳基; R 3和R 4各自独立地表示氢或C 1-6烷基; R 7表示氢或C 1-6烷基; R8表示氢或C1-6烷基;其盐和溶剂合物;是CCR3拮抗剂，因此被认为可用于治疗。

6. 发明申请

WO2003082834A3 MORPHOLINE DERIVATIVES AND INTERMEDIATES THEREFOR 审中-公开
公开(公告)号：WO2003082834A3
公开(公告)日：2003-10-09
申请号：PCT/EP2003/003338
申请日：2003-03-27
申请人： GLAXO GROUP LIMITED , ANCLIFF, Rachael, Ann , COOK, Caroline, Mary , ELDRED, Colin, David , GORE, Paul, Martin , HARRISON, Lee, Andrew , HAYES, Martin, Alistair , HODGSON, Simon, Teanby , JUDD, Duncan, Bruce , KEELING, Suzanne, Elaine , LEWELL, Xiao, Qing , MILLS, Gail , ROBERTSON, Graeme, Michael , SWANSON, Stephen , WALKER, Andrew, John , WILKINSON, Mark
发明人： ANCLIFF, Rachael, Ann , COOK, Caroline, Mary , ELDRED, Colin, David , GORE, Paul, Martin , HARRISON, Lee, Andrew , HAYES, Martin, Alistair , HODGSON, Simon, Teanby , JUDD, Duncan, Bruce , KEELING, Suzanne, Elaine , LEWELL, Xiao, Qing , MILLS, Gail , ROBERTSON, Graeme, Michael , SWANSON, Stephen , WALKER, Andrew, John , WILKINSON, Mark
IPC分类号： C07D265/30
摘要： Compound of formula (I); which is;3-({[({[(2S)-4-(3,4-dichlorobenzyl)morpholin-2-yl]methyl}amino)carbonyl]--amino}methyl)-N-ethylbenzamide;and salts and solvates thereof, a process for its preparation, pharmaceutical formulations containing it and its use in therapy.

7. 发明申请

WO2003082834A2 NOVEL COMPOUND 审中-公开
标题翻译：新型化合物
公开(公告)号：WO2003082834A2
公开(公告)日：2003-10-09
申请号：PCT/EP2003/003338
申请日：2003-03-27
申请人： GLAXO GROUP LIMITED , ANCLIFF, Rachael, Ann , COOK, Caroline, Mary , ELDRED, Colin, David , GORE, Paul, Martin , HARRISON, Lee, Andrew , HAYES, Martin, Alistair , HODGSON, Simon, Teanby , JUDD, Duncan, Bruce , KEELING, Suzanne, Elaine , LEWELL, Xiao, Qing , MILLS, Gail , ROBERTSON, Graeme, Michael , SWANSON, Stephen , WALKER, Andrew, John , WILKINSON, Mark
发明人： ANCLIFF, Rachael, Ann , COOK, Caroline, Mary , ELDRED, Colin, David , GORE, Paul, Martin , HARRISON, Lee, Andrew , HAYES, Martin, Alistair , HODGSON, Simon, Teanby , JUDD, Duncan, Bruce , KEELING, Suzanne, Elaine , LEWELL, Xiao, Qing , MILLS, Gail , ROBERTSON, Graeme, Michael , SWANSON, Stephen , WALKER, Andrew, John , WILKINSON, Mark
IPC分类号： C07D265/30
CPC分类号： C07D265/30
摘要： Compound of formula (I); which is;3-({[({[(2S)-4-(3,4-dichlorobenzyl)morpholin-2-yl]methyl}amino)carbonyl]--amino}methyl)-N-ethylbenzamide;and salts and solvates thereof, a process for its preparation, pharmaceutical formulations containing it and its use in therapy.
摘要翻译：式（I）化合物; 其是3 - （{[（{[（2S）-4-（3,4-二氯苄基）吗啉-2-基]甲基}氨基）羰基] - 氨基}甲基）-N-乙基苯甲酰胺; 其溶剂合物，其制备方法，含有它的药物制剂及其在治疗中的用途。

8. 发明申请

WO2003082291A1 N-{´ (2S) -4- (3, 4-DIFLUOROBENZYL) MORPHOLIN-2YL!METHYL} -2-{3-' (METHYLSULPHONYL) AMINO! PHENYL}ACETAMIDE AS CCR3 ANTAGONIST FOR THE TREATMENT OF INFLAMMATORY CONDITIONS 审中-公开
标题翻译： N- {'（2S）-4-（3,4-二氟硼酸）吗啉-2-基甲基} -2- {3-（甲基磺酰基）氨基] PHENYL}乙酰胺作为治疗炎症条件的CCR3拮抗剂
公开(公告)号：WO2003082291A1
公开(公告)日：2003-10-09
申请号：PCT/EP2003/003339
申请日：2003-03-27
申请人： GLAXO GROUP LIMITED , ANCLIFF, Rachael, Ann , COOK, Caroline, Mary , ELDRED, Colin, David , GORE, Paul, Martin , HARRISON, Lee, Andrew , HAYES, Martin, Alistair , HODGSON, Simon, Teanby , JUDD, Duncan, Bruce , KEELING, Suzanne, Elaine , LEWELL, Xiao, Qing , MILLS, Gail , ROBERTSON, Graeme, Michael , SWANSON, Stephen , WALKER, Andrew, John , WILKINSON, Mark
发明人： ANCLIFF, Rachael, Ann , COOK, Caroline, Mary , ELDRED, Colin, David , GORE, Paul, Martin , HARRISON, Lee, Andrew , HAYES, Martin, Alistair , HODGSON, Simon, Teanby , JUDD, Duncan, Bruce , KEELING, Suzanne, Elaine , LEWELL, Xiao, Qing , MILLS, Gail , ROBERTSON, Graeme, Michael , SWANSON, Stephen , WALKER, Andrew, John , WILKINSON, Mark
IPC分类号： A61K31/5375
CPC分类号： C07D265/30 , A61K31/5375
摘要： Compound of formula (I): HsC H H '(0) IIZZ V which is; 3-(f [({[(2S)-4-(3,4-dichlorobenzyl)morpholin-2-yl]methyl}amino)carbonyl]-amino}methyl)=Nethlylbenzamide; and salts and solvates thereof, a process for its preparation intermediates, pharmaceutical formulations containing it and its use in therapy, as CCR3=antagonist for the treatment of inflammatory conditions.
摘要翻译：式（I）化合物：HsC H H'（O）IIZZ V其为 3-（f [（{[（2S）-4-（3,4-二氯苄基）吗啉-2-基]甲基}氨基）羰基] - 氨基}甲基）=苯基苯甲酰胺; 其盐和溶剂合物，其制备中间体的方法，含有它的药物制剂及其在治疗中的用途，作为CCR3 =用于治疗炎性病症的拮抗剂。

9. 发明申请

WO2003082863A1 N-(MORPHOLIN-2YL) METHYL ACETAMIDE DERIVATIVES AS CCR-3 ANTAGONISTS USEFUL IN THE TREATMENT OF INFLAMMATORY DISEASES 审中-公开
标题翻译： N-（MORPHOLIN-2YL）甲基乙酰胺衍生物作为用于治疗炎症疾病的CCR-3拮抗剂
公开(公告)号：WO2003082863A1
公开(公告)日：2003-10-09
申请号：PCT/EP2003/003350
申请日：2003-03-27
申请人： GLAXO GROUP LIMITED , ANCLIFF, Rachael, Ann , COOK, Caroline, Mary , ELDRED, Colin, David , GORE, Paul, Martin , HARRISON, Lee, Andrew , HAYES, Martin, Alistair , HODGSON, Simon, Teanby , JUDD, Duncan, Bruce , KEELING, Suzanne, Elaine , LEWELL, Xiao, Qing , MILLS, Gail , ROBERTSON, Graeme, Michael , SWANSON, Stephen , WALKER, Andrew, John , WILKINSON, Mark
发明人： ANCLIFF, Rachael, Ann , COOK, Caroline, Mary , ELDRED, Colin, David , GORE, Paul, Martin , HARRISON, Lee, Andrew , HAYES, Martin, Alistair , HODGSON, Simon, Teanby , JUDD, Duncan, Bruce , KEELING, Suzanne, Elaine , LEWELL, Xiao, Qing , MILLS, Gail , ROBERTSON, Graeme, Michael , SWANSON, Stephen , WALKER, Andrew, John , WILKINSON, Mark
IPC分类号： C07D413/12
CPC分类号： C07D413/12
摘要： Compounds of formula (I); wherein: R 1 represents substituted or unsubstituted heterocyclyl; Y represents -(CR na R nb ) n -; R na and R nb are each independently hydrogen or C 1-6 alkyl; n is an integer from 1 to 5; R 2 represents unsubstituted or substituted aryl or unsubstituted or substituted heteroaryl; R 3 represents hydrogen or C 1-6 alkyl; and salts and solvates thereof are CCR-3 antagonists and are thus indicated to be useful in therapy.
摘要翻译：式（I）化合物; 其中：R 1表示取代或未取代的杂环基; Y表示 - （CRnaRnb）n-; Rna和Rnb各自独立地为氢或C 1-6烷基; n为1〜5的整数; R 2表示未取代或取代的芳基或未取代或取代的杂芳基; R 3表示氢或C 1-6烷基; 其盐和溶剂合物是CCR-3拮抗剂，因此被认为可用于治疗。

10. 发明申请

WO2003082294A1 MORPHOLINE DERIVATIVES WITH A SUBSTITUTED ACETAMIDE GROUP IN THE 2-POSITION FOR USE AS CCR-3 ANTAGONISTS FOR THE TREATMENT OF INFLAMMATORY DISEASES 审中-公开
标题翻译：在用于治疗炎症疾病的CCR-3拮抗剂的2位置中具有取代的乙酰胺基团的吗啉衍生物
公开(公告)号：WO2003082294A1
公开(公告)日：2003-10-09
申请号：PCT/EP2003/003348
申请日：2003-03-27
申请人： GLAXO GROUP LIMITED , ANCLIFF, Rachael, Ann , COOK, Caroline, Mary , ELDRED, Colin, David , GORE, Paul, Martin , HARRISON, Lee, Andrew , HAYES, Martin, Alistair , HODGSON, Simon, Teanby , JUDD, Duncan, Bruce , KEELING, Suzanne, Elaine , LEWELL, Xiao, Qing , MILLS, Gail , ROBERTSON, Graeme, Michael , SWANSON, Stephen , WALKER, Andrew, John , WILKINSON, Mark
发明人： ANCLIFF, Rachael, Ann , COOK, Caroline, Mary , ELDRED, Colin, David , GORE, Paul, Martin , HARRISON, Lee, Andrew , HAYES, Martin, Alistair , HODGSON, Simon, Teanby , JUDD, Duncan, Bruce , KEELING, Suzanne, Elaine , LEWELL, Xiao, Qing , MILLS, Gail , ROBERTSON, Graeme, Michael , SWANSON, Stephen , WALKER, Andrew, John , WILKINSON, Mark
IPC分类号： A61K31/5377
CPC分类号： C07D209/48 , C07D265/30 , C07D413/06 , C07D413/12
摘要： Certain compounds of formula (I); wherein R 1 represents substituted or unsubstituted aryl; X represents -O- or a bond; Y represents -(CR na ,R nb ) n-; R na and R nb are each independently hydrogen or C 1-6 alkyl; n is an integer from 1 to 5; R 2 represents unsubstituted or substituted aryl or unsubstituted or substituted heteroaryl; R 3 represents hydrogen or C 1 - 6 alkyl; R 10 represents hydrogen or C 1-6 alkyl; and salts and solvates thereof are CCR3 antagonists and are therefore indicated to be useful in therapy of inflammatory conditions.
摘要翻译：某些式（I）化合物; 其中R1表示取代或未取代的芳基; X表示-O-或键; Y表示 - （CRna，Rnb）n-; Rna和Rnb各自独立地为氢或C 1-6烷基; n为1〜5的整数; R 2表示未取代或取代的芳基或未取代或取代的杂芳基; R 3表示氢或C 1-6烷基; R 10表示氢或C 1-6烷基; 其盐和溶剂合物是CCR3拮抗剂，因此被认为可用于治疗炎性病症。

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