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1. 发明申请

WO2007068929A1 CYCLIC AMINE DERIVATIVES AND THEIR USES 审中-公开
标题翻译：循环胺衍生物及其用途
公开(公告)号：WO2007068929A1
公开(公告)日：2007-06-21
申请号：PCT/GB2006/004675
申请日：2006-12-14
申请人： ARGENTA DISCOVERY LTD. , FINCH, Harry , RAY, Nicholas, Charles , BODIL VAN NIEL, Monique , SMITH, Phillip
发明人： FINCH, Harry , RAY, Nicholas, Charles , BODIL VAN NIEL, Monique , SMITH, Phillip
IPC分类号： C07C271/38 , C07C217/52 , C07C219/24 , C07D311/86 , C07D333/24 , A61K31/27 , A61K31/381 , A61K31/14 , A61K31/216 , A61K31/352 , A61P11/00
CPC分类号： C07C271/38 , C07C217/52 , C07C219/24 , C07C2602/42 , C07D311/86 , C07D333/24
摘要： Compounds of formula (I) have muscarinic M3 receptor modulating activity; formula (I) wherein R 1 is C 1 -C 6 -alkyl or a hydrogen atom; and R 2 is a hydrogen atom or a group -R 5 , or a group, -Z-Y-R 5 , or a group -Z-NR 9 R 10 , or a group -Z-N(R 9 )C(O)R 11 ; and R 3 is a lone pair, or C 1 -C 6 -alkyl; R 4 is selected from one of the groups of formula (a), (b), (c) or (d); formulae (a), (b), (c), (d), Z is a C 1 -C 16 -alkylene, C 2 -C 16 -alkenylene or C 2 -C 16 -alkynylene group; Y is a bond or oxygen atom; R 5 is an C 1 -C 6 -alkyl, aryl, arylalkyl; aryl-fused-cycloalkyl, aryl-fused- heterocycloalkyl, heteroaryl, aryl(C 1 -C 8 -alkyl)-, heteroaryl(C 1 -C 8 -alkyl)-, cycloalkyl or heterocycloalkyl group; R 6 is C 1 -C 6 -alkyl or a hydrogen atom; R 7a and R 7b are a C 1 -C 6 - alkyl group or halogen; n and m are independently 0, 1 , 2 or 3; R 8a and R 8b are independently selected from the group consisting of aryl, aryl-fused-heterocycloalkyl, heteroaryl, C 1 -C 6 -alkyl, cycloalkyl and hydrogen; R 8c is -OH, C 1 -C 6 -alkyl, hydroxy-C 1 -C 6 -alkyl, or a hydrogen atom; R 8d is C 1 -C 6 -alkyl or a hydrogen atom; R 9 and R 10 are independently a hydrogen atom, C 1 -C 6 -alkyl, aryl, aryl-fused-heterocycloalkyl, aryl- fused-cycloalkyl, heteroaryl, aryl(C 1 -C 6 -alkyl)-, or heteroaryl(C 1 -C 6 -alkyl)- group; or R 9 and R 10 together with the nitrogen atom to which they are attached form a heterocyclic ring of 4-8 atoms, optionally containing a further nitrogen or oxygen atom; R 11 is C 1 -C 6 -alkyl or a hydrogen atom; Ar 1 is aryl, heteroaryl or cycloalkyl; Ar 2 are independently aryl, heteroaryl or cycloalkyl; and Q is an oxygen atom, -CH 2 -, -CH 2 CH 2 - or a bond.
摘要翻译：式（I）化合物具有毒蕈碱M3受体调节活性; 式（I）其中R 1是C 1 -C 6 - 烷基或氢原子; 和R 2是氢原子或基团-R 5或基团-ZYR 5或基团-Z-NR 或者是基团-ZN（R 9）C（O）R 11; 且R 3是一对或C 1 -C 6 - 烷基; R 4选自式（a），（b），（c）或（d）中的一个：式（a），（b），（c），（d），Z是C 1 -C 16 - 亚烷基，C 2 -C 16 - 亚烯基或C 2 -C 16 - 亚炔基; Y是键或氧原子; R 5是C 1 -C 6 - 烷基，芳基，芳基烷基; 芳基 - 稠合环烷基，芳基 - 稠合 - 杂环烷基，杂芳基，芳基（C 1 -C 8 - 烷基） - ，杂芳基（C 1 -C 12 - -C≡8烷 - 烷基） - ，环烷基或杂环烷基; R 6是C 1 -C 6 - 烷基或氢原子; R 7a和R 7b是C 1 -C 6 - 烷基或卤素; n和m独立地为0,1,2或3; R 8a和R 8b独立地选自芳基，芳基 - 稠合 - 杂环烷基，杂芳基，C 1 -C 3 烷基，环烷基和氢; R 8c是-OH，C 1 -C 6 - 烷基，羟基-C 1 -C 3 > 6个 - 烷基或氢原子; R 8是C 1 -C 6 - 烷基或氢原子; R 9和R 10独立地是氢原子，C 1 -C 6 - 烷基，芳基，芳基 - 杂芳基（C 1 -C 6 - 烷基） - 或杂芳基（C 1 -C 6 - 烷基） - 杂芳基（C 1 -C 6 - -C 6 -C 6 - 烷基） - 基; 或R 9和R 10与它们所连接的氮原子一起形成4-8个原子的杂环，任选地含有另外的氮或氧原子; R 11是C 1 -C 6 - 烷基或氢原子; Ar 1是芳基，杂芳基或环烷基; Ar 2独立地是芳基，杂芳基或环烷基; 和Q是氧原子，-CH 2 - ， - CH 2 CH 2 - 或键。

2. 发明申请

WO2008096128A1 OXAZOLE AND THIAZOLE DERIVATIVES AND THEIR USES 2 审中-公开
标题翻译：奥扎唑和噻唑衍生物及其用途2
公开(公告)号：WO2008096128A1
公开(公告)日：2008-08-14
申请号：PCT/GB2008/000406
申请日：2008-02-06
申请人： ARGENTA DISCOVERY LTD , FINCH, Harry , RAY, Nicholas, Charles , BULL, Richard, James , BRAVO, Jose, Antonio , AVITABILE, Barbara, Giuseppina
发明人： FINCH, Harry , RAY, Nicholas, Charles , BULL, Richard, James , BRAVO, Jose, Antonio , AVITABILE, Barbara, Giuseppina
IPC分类号： C07D263/32 , A61K31/421 , A61P11/06
CPC分类号： C07D263/32
摘要： Compounds of formula (I): wherein A, X, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 and R 8 are as defined in the Specification are useful in the treatment of diseases where enhanced M3 receptor activation is implicated, such as respiratory tract diseases.
摘要翻译：式（I）化合物：其中A，X，R 1，R 2，R 3，R 4， >，R 5，R 6和R 8如本说明书中所定义，可用于治疗增强M3受体活化的疾病牵连，如呼吸道疾病。

3. 发明申请

WO2007031747A1 IMDOLIZINE DERIVATIVES AS LIGANDS OF THE CRTH2 RECEPTOR 审中-公开
标题翻译：作为CRTH2受体配体的咪唑啉衍生物
公开(公告)号：WO2007031747A1
公开(公告)日：2007-03-22
申请号：PCT/GB2006/003394
申请日：2006-09-14
申请人： ARGENTA DISCOVERY LTD. , HYND, George , RAY, Nicholas, Charles , FINCH, Harry , MONTANA, John, Gary , CRAMP, Michael, Colin , HARRISON, Trevor, Keith , ARIENZO, Rosa , BLANEY, Paul , GRIFFON, Yann , MIDDLEMISS, David
发明人： HYND, George , RAY, Nicholas, Charles , FINCH, Harry , MONTANA, John, Gary , CRAMP, Michael, Colin , HARRISON, Trevor, Keith , ARIENZO, Rosa , BLANEY, Paul , GRIFFON, Yann , MIDDLEMISS, David
IPC分类号： C07D471/04 , A61K31/437 , A61P11/00
CPC分类号： C07D471/04
摘要： Compounds of formula (I) are CRTH2 antagonists, useful in the treatment of, for example, asthma, chronic obstructive pulmonary disease, rhinitis, allergic airway syndrome, and allergic rhinobronchitis. Formula (I) wherein R 1 , R 2 . R 3 and R 4 each independently are hydrogen, C 1 -C 6 alkyl, fully or partially fluorinated C 1 -C 6 alkyl, halo, -S(O) n R 10, -SO 2 N(R 10 ) 2, -N(R 10 ) 2, -C(O)N(R 10 ) 2, -NR 10 C(O)R 9, -CO 2 R 10 , -C(O)R 9 , -NO 2, -CN or -OR 11 ; wherein each R 9 is independently C 1 -C 6 alkyl, aryl, heteroaryl; R 10 is independently hydrogen, C 1 -C 6 alkyl, aryl, or heteroaryl; R 11 is hydrogen, C 1 -C 6 alkyl, fully or partially fluorinated C 1 -C 6 alkyl or a group -SO 2 R 10 ; n is 0, 1 or 2; R 5 is C 1 -C 6 alkyl, fully or partially fluorinated C 1 -C 6 alkyl, C 1 -C 6 alkenyl, C 1 -C 6 alkynyl, optionally substituted aryl, or optionally substituted heteroaryl; R 6 is hydrogen, C 1 -C 6 alkyl or fully or partially fluorinated C 1 -C 6 alkyl ; R 7 and R 8 are independently hydrogen or C 1 -C 6 alkyl, or R 7 and R 8 together with the atom to which they are attached form a cycloalkyl group; and X is -CHR 6 -, -S(O) n -, -C(O)-, -NR 6 SO 2 - or -SO 2 NR 6 - wherein n is 0, 1 or 2.
摘要翻译：式（I）化合物是CRTH2拮抗剂，可用于治疗例如哮喘，慢性阻塞性肺病，鼻炎，过敏性气道综合征和过敏性鼻炎支原体炎。式（I）其中R 1，R 2， R 3和R 4各自独立地是氢，C 1 -C 6烷基，完全或部分氟化的C C 1 -C 6烷基，卤素，-S（O）n R 10，-SO 2 - ， - 2 N（R 10）2，-N（R 10）2， - C （O）N（R 10）2，-NR 10 C（O）R 9，-CO -C（O）R 9，-NO 2，-CN或-OR 2， SUB> 11 ; 其中每个R 9独立地是C 1 -C 6烷基，芳基，杂芳基; R 10独立地是氢，C 1 -C 6 -C 6烷基，芳基或杂芳基; R 11是氢，C 1 -C 6烷基，完全或部分氟化的C 1 -C 3 > 6个或多个烷基或基团-SO 2 R 10; n为0,1或2; R 5是C 1 -C 6烷基，完全或部分氟化C 1 -C 6烷基，C 1 -C 6烷基，C 1 -C 6烷基，C 1 -C 6烷基， C 1 -C 6烷基，C 1 -C 6亚烯基，C 1 -C 6 - 炔基，任选取代的芳基或任选取代的杂芳基; R 6是氢，C 1 -C 6烷基或完全或部分氟化的C 1 -C 3 > 6个烷基; R 7和R 8独立地是氢或C 1 -C 6烷基，或R 7 R 3和R 8与它们所连接的原子一起形成环烷基; 并且X是-CHR 6 - ， - S（O）n - ， - C（O） - ， - NR 6 SO > 2 - 或-SO 2 NR 6 - ，其中n为0,1或2。

4. 发明申请

WO2007017669A1 AZOLE AND THIAZOLE DERIVATIVES AND THEIR USE 审中-公开
标题翻译：偶氮和噻唑衍生物及其用途
公开(公告)号：WO2007017669A1
公开(公告)日：2007-02-15
申请号：PCT/GB2006/002956
申请日：2006-08-08
申请人： ARGENTA DISCOVERY LTD. , RAY, Nicholas, Charles , BULL, Richard, James , FINCH, Harry , VAN DEN HEUVEL, Marco , BRAVO, Jose, Antonio
发明人： RAY, Nicholas, Charles , BULL, Richard, James , FINCH, Harry , VAN DEN HEUVEL, Marco , BRAVO, Jose, Antonio
IPC分类号： C07D263/32 , C07D277/30 , A61K31/421 , A61K31/426
CPC分类号： C07D263/32 , C07D277/28 , C07D413/06 , C07D413/12
摘要： Compounds of formula (I) are useful in the treatment of diseases where enhanced M3 receptor activation is implicated, such as respiritory tract diseases: wherein (i) R 1 is C 1 -C 6 -alkyl or hydrogen; and R 2 is hydrogen or a group -R 7 , -Z-Y-R 7 , -Z-NR 9 R 10 ; -Z-CO-NR 9 R 10 , -Z-NR 9 - [AE11] C(O)O-R 7 , or -Z-C(O)-R 7 ; and R 3 is a lone pair, or C 1 C 6 -alkyl; or (ii) R 1 and R 3 together with the nitrogen to which they are attached form a heterocycloalkyl ring, and R 2 is a lone pair or a group -R 7 , -Z-Y-R 7 , -Z-NR 9 R 10 , -Z-CO-NR 9 R 10 , -Z-NR 9 - [AE12] C(O)O-R 7 ; or; -Z-C(O)-R 7 ; or (iii) R 1 and R 2 together with the nitrogen to which they are attached form a heterocycloalkyl ring, said ring being substituted by a group -Y-R 7 , -Z-Y-R 7 , -Z-NR 9 R 10 ; -Z-CO-NR 9 R 10 ; -Z-NR 9 - [AE13] C(O)O-R 7 ; or; -Z-C(O)-R 7 ; and R 3 is a lone pair, or C 1 -C 6 -aIkyl; R 4 and R 5 are independently selected from the group consisting of aryl, arytfused-heterocycloalkyl, heteroaryl, C 1 -C 6 -alkyl, cycloalkyl; R 6 is -OH, C 1 -C 6 -alkyl, C 1 -C 6 -alkoxy, hydroxy-C 1 -C 6 -alkyl, nitrile, a group CONR 8 2 or a hydrogen atom; A is an oxygen or a sulfur atom; X is an alkylene, alkenylene or alkynylene group; R 7 is an C 1 -C 6 -alkyl, aryl, aryl-fused-cycloalkyl, aryl-ffused-heterocycloalkyl, heteroaryl, aryl(C 1 -C 8 -alkyl)-, heteroaryl(C 1 -C 8 -alkyl)-, cycloalkyl or heterocycloalkyl group; R 8 is C 1 -C 6 -alkyl or a hydrogen atom; Z is a C 1 -C 16 -alkylene, C 2 -C 16 -alkenylene or C 2 -C 16 -alkynylene group; Y is a bond or oxygen atom; R 9 and R 10 are independently a hydrogen atom, C 1 -C 6 -alkyl, aryl, aryl-fused-heterocycloalkyl, aryl-fused-cycloalkyl, heteroaryl, aryl(C 1 -C 6 -alkyl)-, or heteroaryl(C 1 -C 6 -alkyl)- group; or R 9 and R 10 together with the nitrogen atom to which they are attached form a heterocyclic ring of 48 atoms, optionally containing a further nitrogen or oxygen atom.
摘要翻译：式（I）化合物可用于治疗涉及增强的M3受体激活的疾病，例如呼吸道疾病：其中（i）R 1是C 1〜 -C 6 - 烷基或氢; R 2是氢或基团-R 7，-ZYR 7，-Z-NR 9 R ^{10 ; -Z-CO-NR 9 R 10，-Z-NR 9 - - - - - - ）或或-ZC（O）-R 7; 且R 3是单对或C 1 -C 6 - 烷基; 或（ii）R 1和R 3与它们所连接的氮一起形成杂环烷基环，并且R 2是孤立的对或基团-R 7，-ZYR 7，-Z-NR 9 R 10，-Z -CO-NR 9 R 10，-Z-NR 9 - - - - - - （C）O（O）OR ^{7 ; 要么; -Z-C（O）-R ^{7 ; 或（iii）R 1和R 2与它们所连接的氮一起形成杂环烷基环，所述环被基团-YR 7 9，-ZYR＆lt; 7＆gt;，-Z-NR 9＆lt; 10＆gt; -Z-CO-NR ^{9 - [R ^{10 ; -Z-NR ^{9 - _{[AE13] C（O）O-R ^{7 ; 要么; -Z-C（O）-R ^{7 ; 且R 3是一对或C 1 -C 6 - 烷基; R 4和R 5独立地选自芳基，芳基 - 杂环烷基，杂芳基，C 1 -C 6 烷基，环烷基; R 6是-OH，C 1 -C 6 - 烷基，C 1 -C 6 烷氧基，羟基-C 1 -C 6 - 烷基，腈，CONR 8 -}}}}}}}}}

5. 发明申请

WO2008149053A1 BICYCL0 [2. 2. 1] HE PT- 2-YLAMINE DERIVATES AND THEIR USE 审中-公开
标题翻译： BICYCL0 [2。 2. 1] PT-2-氨基衍生物及其用途
公开(公告)号：WO2008149053A1
公开(公告)日：2008-12-11
申请号：PCT/GB2007/002130
申请日：2007-06-08
申请人： ARGENTA DISCOVERY LTD. , ASTRAZENECA AB , FINCH, Harry , JENNINGS, Andrew, Stephan, Robert , van NIEL, Monique, Bodil , RAY, Nicholas, Charles , SMITH, Philip
发明人： FINCH, Harry , JENNINGS, Andrew, Stephan, Robert , van NIEL, Monique, Bodil , RAY, Nicholas, Charles , SMITH, Philip
IPC分类号： C07C211/38 , C07C211/63 , C07D311/84 , C07D311/86 , C07D333/24 , C07D409/12 , A61K31/216 , A61K31/352 , A61K31/381 , A61P1/00 , A61P9/00 , A61P11/00 , A61P13/00 , A61P37/00
CPC分类号： C07C219/24 , C07C2601/14 , C07C2602/42 , C07C2603/18 , C07D311/82 , C07D333/24 , C07D409/06 , C07D409/14
摘要： A named compound of formula (I): having M3 receptor antagonist activity; a composition comprising such a compound; the use of such a compound in therapy (such as asthma or COPD); and a method of treating a patient with such a compound.
摘要翻译：命名的式（I）化合物：具有M3受体拮抗剂活性; 包含这种化合物的组合物; 在治疗（如哮喘或COPD）中使用这种化合物; 以及用这种化合物治疗患者的方法。

6. 发明申请

WO2008096093A1 OXAZOLE AND THIAZOLE DERIVATIVES AND THEIR USES 审中-公开
标题翻译：奥沙唑和噻唑衍生物及其用途
公开(公告)号：WO2008096093A1
公开(公告)日：2008-08-14
申请号：PCT/GB2007/000395
申请日：2007-02-06
申请人： ARGENTA DISCOVERY LTD. , RAY, Nicholas, Charles , BULL, Richard, James , FINCH, Harry , VAN DEN HEUVEL, Marco , BRAVO, Jose, Antonio
发明人： RAY, Nicholas, Charles , BULL, Richard, James , FINCH, Harry , VAN DEN HEUVEL, Marco , BRAVO, Jose, Antonio
IPC分类号： C07D263/32 , C07D277/28 , C07D413/12 , A61K31/421 , A61K31/426 , A61P11/08
CPC分类号： C07D263/32 , C07D277/28 , C07D413/12
摘要： A quaternary ammonium compound of formula (I) having M3 receptor antagonist activity; a composition comprising such a compound; the use of such a compound in therapy (such as asthma or COPD); and a method of treating a patient with such a compound.
摘要翻译：具有M3受体拮抗剂活性的式（I）季铵化合物; 包含这种化合物的组合物; 在治疗（如哮喘或COPD）中使用这种化合物; 以及用这种化合物治疗患者的方法。

7. 发明申请

WO2007036743A3 QUINOLINES AND THEIR THERAPEUTIC USE 审中-公开
公开(公告)号：WO2007036743A3
公开(公告)日：2007-04-05
申请号：PCT/GB2006/003644
申请日：2006-09-29
申请人： ARGENTA DISCOVERY LTD. , CRAMP, Michael, Colin , ARIENZO, Rosa , HYND, George , CRACKETT, Peter , GRIFFON, Yann , HARRISON, Trevor, Keith , RAY, Nicholas, Charles , FINCH, Harry , MONTANA, John, Gary
发明人： CRAMP, Michael, Colin , ARIENZO, Rosa , HYND, George , CRACKETT, Peter , GRIFFON, Yann , HARRISON, Trevor, Keith , RAY, Nicholas, Charles , FINCH, Harry , MONTANA, John, Gary
IPC分类号： A61K31/47 , A61P11/00 , A61P43/00 , C07D215/00
摘要： Compounds of formula [1] are CRTH2 antagonists, useful in the treatment of conditions having an inflammatory component; in which: R 1 , R 2 , R 3 , R 4 and R 5 are independently hydrogen, C 1 -C 6 alkyl, C 1 - C 6 fluoroalkyl, cyclopropyl, halo, -S(O) n R 6 , -SO 2 NR 7 R 8 , -NR 7 R 8 , -NR 7 C(O)R 6 , -CO 2 R 7 , -C(O)NR 7 R 8 , -C(O)R 6 , -NO 2 , -CN or a group -OR 9 ; wherein each R 6 is independently C 1 -C 6 alkyl, C 1 -C 6 fluoroalkyl, cycloalkyl, aryl, or heteroaryl; R 7 , R 8 are independently C 1 -C 6 alkyl, C 1 -C 6 fluoroalkyl, cycloalkyl, cycloalkyl-(C 1 -C 6 alkyl)-, aryl, heteroaryl or hydrogen; R 9 is hydrogen, C 1 -C 6 alkyl, C 1 -C 6 fluoroalkyl, cycloalkyl, cylcoalkyl-(C 1 -C 6 alkyl)-, or a group -SO 2 R 6 ; A is -CHR 10 -, -C(O)-, -S(O) n -, -0-, or -NR 10 - wherein n is an integer from 0-2 and R 10 is hydrogen, C 1 -C 3 alkyl, or C 1 -C 6 fluoroalkyl group; B is a direct bond, or a divalent radical selected from -CH 2 -, -CH 2 CH 2 -, -CHR 11 -, -CR 11 R 12 -, -CH 2 CHR 11 -, -CH 2 CR 11 R 12 -, -CHR 11 CHR 12 -, and divalent radicals of formula -(CR 11 R 12 ) P -Z- wherein Z is attached to the ring carrying R 1 , R 2 and R 3 ; wherein R 11 is C 1 -C 3 alkyl, cyclopropyl, C 1 -C 6 fluoroalkyl; R 12 is methyl or fluoromethyl; p is independently 1 or 2; and Z is -0-, -NH-, or -S(O) n -, wherein n is an integer from 0-2; X is a carboxylic acid, tetrazole, 3-hydroxyisoxazole, hydroxamic acid, phosphinate, phosphonate, phosphonamide, or sulfonic acid group, or a group of formula C(=O)NHSO 2 R 6 or SO 2 NHC(=O)R 6 ; and Y is aryl, heteroaryl, aryl-fused- heterocycloalkyl, heteroaryl-fused-cycloalkyl, heteroaryl-fused-heterocycloalkyl or aryl-fused-cycloalkyl group.

8. 发明申请

WO2007017670A1 BICYCLO[2.2.]HEPT-7-YLAMINE DERIVATIVES AND THEIR USES 审中-公开
标题翻译： BICYCLO [2.2。] HEPT-7-YLAMINE DERIVATIVES及其用途
公开(公告)号：WO2007017670A1
公开(公告)日：2007-02-15
申请号：PCT/GB2006/002957
申请日：2006-08-08
申请人： ARGENTA DISCOVERY LTD. , FINCH, Harry , RAY, Nicholas, Charles , BULL, Richard, James , van NEIL, Monique, Bodil , JENNINGS, Andrew, Stephen, Robert
发明人： FINCH, Harry , RAY, Nicholas, Charles , BULL, Richard, James , van NEIL, Monique, Bodil , JENNINGS, Andrew, Stephen, Robert
IPC分类号： C07C271/38 , C07C219/24 , C07C233/41 , C07D211/14 , C07D311/84 , C07D311/86 , C07D333/16 , C07D409/14 , A61K31/27 , A61K31/381 , A61K31/451 , A61K31/221 , A61K31/352 , A61K31/4704 , A61P29/00
CPC分类号： C07C271/38 , C07C219/24 , C07C235/36 , C07C2602/42 , C07D211/14 , C07D311/84 , C07D311/86 , C07D333/16 , C07D409/06 , C07D409/14
摘要： Compounds of formula (I) have muscarinic M3 receptor modulating activity; Formula(I) wherein A is an oxygen atom or group -N(R 12 )-;(i) R 1 is C 1 -C 6 -alkyl or a hydrogen atom; and R 2 is a hydrogen atom or a group -R 5 , -Z-Y-R 5 -Z-NR 9 R 10 ; -Z-CO-NR 9 R 10 ; -Z-NR 9 -CO-R 5 ; or -Z-CO 2 H; and R 3 is a lone pair,or C 1 -C 6 -aIkyl in which case the nitrogen atom to which it is attached is a quaternary nitrogen and carries a positive charge; or (ii) R 1 and R 3 together with the nitrogen to which they are attached form a heterocycloalkyl ring, and R 2 is a hydrogen atom; or a group -R 5 , -Z-Y-R 5 , -Z-NR 9 R 10 , -Z-CO-NR 9 R 10 , -Z-NR 9 -CO-R 5 , or -Z-CO 2 H, in which cases the nitrogen atom to which it is attached is a quaternary nitrogen and carries a positive charge; or (iii) R 1 and R 2 together with the nitrogen to which they are attached form a heterocycloalkyl ring, said ring being substituted by a group -Y-R 5 , -Z-Y-R 5 , -Z-NR 9 R 10 ; -Z-CO-NR 9 R 10 ; -Z-NR 9 -CO-R 5 ; or -Z-CO 2 H and R 3 is a lone pair, or C 1 -C 6 -alkyl in which case the nitrogen atom to which it is attached is a quaternary nitrogen and carries a positive charge; R 4 is a group of formula (a), (b), (c) or (d); is an C 1 -C 6 -alkyl, aryl, aryl-fused-cycloalkyl, aryl-fused-heterocycloalkyl, heteroaryl, aryl(C 1 -C 8 -alkyl)-, heteroaryl(C 1- C 8 -alkyl)-, cycloalkyl or heterocycloalkyl group, and the remaining variables are as defined in the specification.
摘要翻译：式（I）化合物具有毒蕈碱M3受体调节活性; 式（I）其中A是氧原子或基团-N（R 12） - ;（i）R 1是C 1 - C 6 - 烷基或氢原子; R 2是氢原子或基团-R 5，-ZYR 5 -Z-NR 9， [R ^{10 ; -Z-CO-NR ^{9 - [R ^{10 ; -Z-NR ^{9 -CO-R ^{5 ; 或-Z-CO 2 H; 且R 3是孤对的或C 1 -C 6 - 烷基，在这种情况下，其所连接的氮原子是季氮并带正电荷; 或（ii）R 1和R 3与它们所连接的氮一起形成杂环烷基环，R 2是氢原子; 或基团-R 5，-ZYR 5，-Z-NR 9，R 10，-Z- CO-NR 9 R 10，-Z-NR 9 -CO-R 5，或-Z- CO 2 H，其中附着的氮原子是季氮并带正电荷; 或（iii）R 1和R 2与它们所连接的氮一起形成杂环烷基环，所述环被基团-YR 5 9，-ZYR 5，-Z-NR 9，R 10， -Z-CO-NR ^{9 - [R ^{10 ; -Z-NR ^{9 -CO-R ^{5 ; 或-Z-CO 2 H和R 3是孤对的或C 1 -C 6 - 烷基，在这种情况下，其所连接的氮原子是季氮并携带正电荷; R 4是式（a），（b），（c）或（d）的基团。是C 1 -C 6 - 烷基，芳基，芳基 - 稠合环烷基，芳基 - 稠合 - 杂环烷基，杂芳基，芳基（C 1〜 C 1 -C 8 - 烷基） - ，杂芳基（C 1 -C 8 - 烷基） - ，环烷基或杂环烷基，剩余的变量如规范中所定义。}}}}}}}}}

9. 发明申请

WO2007045867A1 3 -AMINOINDOLE COMPOUNDS AS CRTH2 RECEPTOR LIGANDS 审中-公开
标题翻译： 3 -AMINOINDOLE化合物作为CRTH2受体配体
公开(公告)号：WO2007045867A1
公开(公告)日：2007-04-26
申请号：PCT/GB2006/003872
申请日：2006-10-18
申请人： ARGENTA DISCOVERY LTD. , RAY, Nicholas, Charles , HYND, George , ARIENZO, Rosa , FINCH, Harry
发明人： RAY, Nicholas, Charles , HYND, George , ARIENZO, Rosa , FINCH, Harry
IPC分类号： C07D209/40 , A61K31/405 , A61P29/00
CPC分类号： C07D209/40
摘要： Compounds of formula [I] are CRTH2 antagonists, useful in the treatment o conditions having an inflammatory component: in which: R 1 , R 2 , R 3 and R 4 are independently hydrogen, (C 1 -C 6 ) alky!, (C 1 -C 6 ) haloalkyl, halo, -S(O) n R 10 , -NR 11 SO 2 R 10 , -SO 2 N(R 11 ) 2 , -N(R 11 ) 2 , -NR 11 C(O)R 10 , -C(O)N(R 11 ) 2 , -CO 2 R 11 , -C(O)R 10 , CN or a group OR 12 ; wherein each R 10 is independently (C 1 -C 6 ) alkyl, (C 1 -C 6 ) haloalkyl, cycloalkyl, aryl, or heteroaryl; R 11 is independently hydrogen, (C 1 -C 6 )alkyl, (C 1 -C 6 ) haloalkyl, cycloalkyl, aryl, or heteroaryl; R 12 is hydrogen, (C 1 -C 6 ) alkyl, (C 1 -C 6 ) haloalkyl, cycloalkyl, or a group -SO 2 R 10 , wherein n is O 1 or 2; R 5 and R 6 are independently hydrogen, (C 1 -C 6 ) alkyl or (C 1 -C 6 ) haloalkyl, or R 5 and R 6 together with the atom to which they are attached form a cycloalkyl group; R 7 is hydrogen, (C 1 -C 6 ) alkyl, or (C 1 -C 6 ) haloalkyl; R 8 is aryl, heteroaryl, aryl-fused-heterocycloalkyl, heteroaryl-fused-cycloalkyl, heteroaryl-fused- heterocycloalkyl or aryl-fused-cycloalkyl; and R 9 is hydrogen, (C 1 -C 6 ) alkyl, (C 1 -C 6 ) haloalkyl, or cycloalkyl.
摘要翻译：式[I]化合物是CRTH2拮抗剂，可用于治疗具有炎性成分的条件：其中：R 1，R 2，R 3， R 4和R 4独立地是氢，（C 1 -C 6）烷基（C 1 -C 6）烷基，卤代烷基，卤素，-S（O）n R 10，-NR 11，SO 2， 2，N 2，N 2，N 2，R 2，R 2， N（R 11）2，-NR 11 C（O）R 10，-C（O） N（R 11）2，-CO 2 R 11，-C（O）R 11， 10，CN或基团OR 12; 其中每个R 10独立地为（C 1 -C 6 -C 6）烷基，（C 1 -C 6 - C 卤代烷基，环烷基，芳基或杂芳基; R 11独立地是氢，（C 1 -C 6 -C 6）烷基，（C 1 -C 6亚烷基）卤代烷基，环烷基，芳基或杂芳基; R 12是氢，（C 1 -C 6 - ）烷基，（C 1 -C 6 - 6个）卤代烷基，环烷基或基团-SO 2 R 10，其中n是O 1或2; R 5和R 6独立地是氢，（C 1 -C 6 -C 6）烷基或（C _{1个C 6 -C 6卤代烷基或R 5和R 6和它们所连接的原子一起形成一个环烷基 R 7是氢，（C 1 -C 6 -C 6）烷基，或（C 1 -C 3 - C > 6个）卤代烷基; R 8是芳基，杂芳基，芳基稠合 - 杂环烷基，杂芳基 - 稠合环烷基，杂芳基 - 稠合 - 杂环烷基或芳基稠合环烷基; 并且R 9是氢，（C 1 -C 6 -C 6）烷基，（C 1 -C 6 - C > 6个）卤代烷基或环烷基。}

10. 发明申请

WO2006082412A2 MULTIMERS OF HETEROCYCLIC COMPOUNDS AND THEIR USE 审中-公开
标题翻译：多元醇的杂环化合物及其用途
公开(公告)号：WO2006082412A2
公开(公告)日：2006-08-10
申请号：PCT/GB2006/000361
申请日：2006-02-03
申请人： ARGENTA DISCOVERY LTD , FINCH, Harry , EDWARDS, Christine , RAY, Nicholas, Charles , O'CONNOR, Elizabeth, Anne , FITZGERALD, Mary, F.
发明人： FINCH, Harry , EDWARDS, Christine , RAY, Nicholas, Charles , O'CONNOR, Elizabeth, Anne , FITZGERALD, Mary, F.
IPC分类号： C07D239/22 , C07D401/12 , C07D403/14 , A61K31/513 , A61P9/00
CPC分类号： C07D239/22 , A61K31/513 , A61K47/55 , C07D401/12 , C07D403/14
摘要： A compound of formula (I): M-L-M, wherein L is a linker and each M is independently a group of formula (II): is useful in therapy, e.g. of respiratory diseases.
摘要翻译：式（I）的化合物：M-L-M，其中L是连接体，每个M独立地是式（II）的基团：可用于治疗，例如，的呼吸系统疾病。

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