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1. 发明申请

WO2008099186A8 HETEROCYCLIC DERIVATIVES AS M3 MUSCARINIC RECEPTORS 审中-公开
标题翻译：作为M3 MUSCARINIC受体的杂环衍生物
公开(公告)号：WO2008099186A8
公开(公告)日：2008-11-13
申请号：PCT/GB2008000519
申请日：2008-02-14
申请人： ARGENTA DISCOVERY LTD , AVITABILE BARBARA GIUSEPPINA , FINCH HARRY , KNIGHT JAMIE DAVID , NADIN ALAN JOHN , RAY NICHOLAS CHARLES
发明人： AVITABILE BARBARA GIUSEPPINA , FINCH HARRY , KNIGHT JAMIE DAVID , NADIN ALAN JOHN , RAY NICHOLAS CHARLES
IPC分类号： C07D471/08 , A61K31/439 , A61P1/00 , A61P9/00 , A61P11/00
CPC分类号： C07D471/08
摘要： This invention relates to M3 antagonists of formula (I) wherein R 2 , R 4 , R 5 , R 6 , W, V, A, D, X, t, u and v are as defined herein; pharmaceutical compositions containing them; methods for their preparation; and their use in the treatment of diseases where enhanced M3 receptor activation is implicated.
摘要翻译：本发明涉及式（I）的M3拮抗剂，其中R 2，R 4，R 5，R 6， >，W，V，A，D，X，t，u和v如本文所定义; 含有它们的药物组合物; 其准备方法; 以及它们用于治疗涉及M3受体活化增强的疾病。

2. 发明申请

WO2007107706A3 DIMERS OF HETEROCYCLIC COMPOUNDS FOR THE TREATMENT OF COPD 审中-公开
标题翻译：用于治疗COPD的异构化合物二聚体
公开(公告)号：WO2007107706A3
公开(公告)日：2008-10-09
申请号：PCT/GB2007000919
申请日：2007-03-16
申请人： ARGENTA DISCOVERY LTD , FINCH HARRY , EDWARDS CHRISTINE , RAY NICHOLAS CHARLES
发明人： FINCH HARRY , EDWARDS CHRISTINE , RAY NICHOLAS CHARLES
IPC分类号： A61K47/48 , A61P11/00 , A61P11/06 , A61P17/00 , A61P17/06 , A61P29/02 , C07D213/82 , C07D401/12 , C07D403/12
CPC分类号： C07D401/12 , A61K47/55 , C07D213/82 , C07D213/85 , C07D401/14 , C07D413/14
摘要： Covalent conjugates of two or more compounds, each having a structure as defined in any of WO2004/043924, WO2005/021509, WO2005/021512, WO2005/026123, WO2005/026124, WO2006/098683 and WO2006/098684, are inhibitors of human neutrophil elastase, useful in treatment of, for example, chronic obstructive pulmonary disease. Dimers of formula (IA) or (IB): wherein LINKER and the variable substituents are particular types of such multimers.
摘要翻译：两种或更多种化合物的共价缀合物，其各自具有如WO2004 / 043924，WO2005 / 021509，WO2005 / 021512，WO2005 / 026123，WO2005 / 026124，WO2006 / 098683和WO2006 / 098684中任一个所定义的结构，是人嗜中性粒细胞抑制剂弹性蛋白酶，可用于治疗例如慢性阻塞性肺疾病。式（IA）或（IB）的二聚体：其中LINKER和可变取代基是这种多聚体的特定类型。

3. 发明申请

WO2006136859A3 INDOLI ZINE DERIVATIVES AND THEIR USE AS CRTH2 ANTAGONISTS 审中-公开
标题翻译：吲哚嗪衍生物及其作为CRTH2拮抗剂的用途
公开(公告)号：WO2006136859A3
公开(公告)日：2007-04-05
申请号：PCT/GB2006002341
申请日：2006-06-26
申请人： ARGENTA DISCOVERY LTD , HYND GEORGE , RAY NICHOLAS CHARLES , FINCH HARRY , MIDDLEMISS DAVID , CRAMP MICHAEL COLIN , BLANEY PAUL MATTHEW , WILLIAMS KAREN , GRIFFON YAN , HARRISON TREVOR KEITH , CRACKETT PETER
发明人： HYND GEORGE , RAY NICHOLAS CHARLES , FINCH HARRY , MIDDLEMISS DAVID , CRAMP MICHAEL COLIN , BLANEY PAUL MATTHEW , WILLIAMS KAREN , GRIFFON YAN , HARRISON TREVOR KEITH , CRACKETT PETER
IPC分类号： C07D471/04 , A61K31/437 , A61P11/06 , A61P11/08 , A61P17/00 , A61P19/02 , A61P29/00 , A61P37/08
CPC分类号： C07D471/04
摘要： Compounds of formula (I) are ligands of the CRTH2 receptor and are useful in the treatment of respiratory disease: 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 9 ; n is 0, 1 or 2; R5 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 -, -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受体的配体，可用于治疗呼吸系统疾病：式（I）其中R 1，R 2，R 2， > 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 1 烷基，卤素，-S（O）n R 10，-SO 2 N， N（R 10）2，-N（R 10）2 - ， - C（O）N（R 10） R 10，-NR 10 C（O）R 9，-CO 2， -C（O）R 9，-NO 2，-CN或-OR 11， SUB>; 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C 1 -C 6 烷基或基团-SO 2 R 9; 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， 1个C 6链烯基，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 6 烷基; R 7和R 8独立地是氢或C 1 -C 6烷基，或R 7， / SUB和R 8与它们所连接的原子一起形成环烷基; 和X是-CHR 6 - ， - S（O）n - ， - NR 6 SO 2 - 或-SO 2 NR 6 - ，其中n为0,1或2。

4. 发明申请

WO2007036743A2 QUINOLINES AND THEIR THERAPEUTIC USE 审中-公开
标题翻译： QUINOLINES及其治疗用途
公开(公告)号：WO2007036743A2
公开(公告)日：2007-04-05
申请号：PCT/GB2006003644
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
CPC分类号： C07D215/233 , A61K31/47 , C07D215/12 , C07D215/18 , C07D215/20 , C07D215/227 , C07D215/36 , C07D215/48 , C07D401/04 , C07D401/10 , C07D401/12
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.
摘要翻译：式[1]化合物是CRTH2拮抗剂，可用于治疗具有炎性组分的病症; 其中：R 1，R 2，R 3，R 4，R 5，R 5，R 5，R 5，其中R 1独立地为氢，C 1 -C 6烷基，C 1 -C 6烷基，氟代烷基，环丙基，卤素，-S（O）n R 6，-SSO 2，NR 7，R 8，（O）R 6，-CO，-CONR 8，-CONR 8，-CONR 8，（O）NR 7，R 8，-C（O）R 8，-C（O）R 9， -NO 2，-CN或基团-OR 9; 其中每个R 6独立地为C 1 -C 6烷基，C 1 -C 6烷基，氟代烷基，环烷基，芳基或杂芳基; R 7，R 8独立地为C 1 -C 6烷基，C 1 SUB （C 1 -C 6烷基） - ，芳基，杂芳基或氢; R 9为氢，C 1 -C 6烷基，C 1 -C 6烷基，C 1 -C 6烷基，（C 1 -C 6烷基） - 或基团-SO 2 SUB 6 R 6， ; A是-CHR 10 - ， - C（O） - ， - S（O）n - ， - O-或-NR 10 10 其中n是0-2的整数，并且R 10是氢，C 1 -C 3烷基或C 1 -C 4烷基， 1 -C 6氟代烷基; B是直接键或选自以下的二价基团：-CH 2 - ， - CH 2 SUBCH 2 - ， - CHR 2 CON - 11 - ， - CR 11， - CH 2， - CH 2 - ， - CH 2 - ， - CH 2，-CH 2，CH 2，CHR 12，CH 2 CH 2，CH 2 CH 2，CH 2 CH 2，和式 - （CR 11 R 12）的二价基团其中Z连接到携带R 1的环上 R＆lt; SUP＆gt;和R＆lt; 3＆gt;; 其中R 11为C 1 -C 3烷基，环丙基，C 1 -C 6烷基，C 1 -C 4烷基， / SUB>氟烷基; R 12是甲基或氟甲基; p独立地为1或2; 和Z是-O - ， - NH-或-S（O）n - ，其中n是0-2的整数; X为羧酸，四唑，3-羟基异恶唑，异羟肟酸，次膦酸酯，膦酸酯，膦酰胺或磺酸基，或式C（= O）NHSO 2 R 6 或SO 2，NHC（= O）R 6，且Y为芳基，杂芳基，芳基稠合的杂环烷基，杂芳基稠合的环烷基，杂芳基稠合的杂环烷基或芳基稠合的环烷基。

5. 发明申请

WO2006082412A3 MULTIMERS OF PYRIMIDINONE DERIVATIVES AND THEIR USE AS HUMAN NEUTROPHIL ELASTASE INHIBITORS 审中-公开
标题翻译：多聚赖氨酸衍生物及其作为人类中性粒细胞抑制剂的用途
公开(公告)号：WO2006082412A3
公开(公告)日：2006-10-12
申请号：PCT/GB2006000361
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 , A61K31/513 , A61P9/00 , C07D401/12 , C07D403/14
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是连接基，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。

6. 发明专利

BRPI0721477A2 未知
公开(公告)号：BRPI0721477A2
公开(公告)日：2013-01-15
申请号：BRPI0721477
申请日：2007-03-21
申请人： ARGENTA DISCOVERY LTD
发明人： HYND GEORGE , GRIFFON YANN , MIDDLEMISS DAVID , RAY NICHOLAS CHARLES , FINCH HARRY , MONTANA JOHN GARY , CRAMP MICHAEL COLIN , HARRISON TREVOR KEITH , ARIENZO ROSA , BLANEY PAUL
IPC分类号： A61K31/437 , A61P11/00 , C07D471/04
摘要： The specific compounds of this list: {7-cyano-2-methyl-1-[4-(morpholine-4-sutfonyl)benzyl]indolizin-3-yl}acetic acid, {1-(3-chloro-4-ethanesulfonylbenzyl)-7-cyano-2-methylindolizin-3-yl}acetic acid, {1-[3-chloro4-(morpholine-4-sulfonyl)benzyl]-7-cyano-2-methylindolizin-3-yl}acetic acid, {1-(3-chloro-4-ethanesulfonylphenylsulfanyl)-7-cyano-2-methylindolizin-3-yl}acetic acid, {1-[3-chloro-4-(morpholine-4-sutfonyl)phenylsutfanyl]-7-cyano-2-methylindolizin-3-yl}acetic acid, {7-cyano-1-(6-fluoroquinolin-2-ylmethyl)-2-methylindolizin-3-yl}acetic acid are ligands of the CRTH2 receptor and are useful in the treatment of respiratory diseases.

7. 发明专利

UA95255C2 未知
公开(公告)号：UA95255C2
公开(公告)日：2011-07-25
申请号：UAA200802945
申请日：2006-08-08
申请人： ARGENTA DISCOVERY LTD
发明人： RAY NICHOLAS CHARLES , BULL RICHARD JAMES , FINCH HARRY , VAN DEN HEUVEL MARCO , BRAVO JOSE ANTONIO
IPC分类号： C07D263/32 , A61K31/421 , A61K31/426 , C07D277/28 , C07D277/30 , C07D413/06 , C07D413/12

8. 发明专利

NZ566068A Bicyclo[2.2.1]hept-7-ylamine derivatives and their uses 未知
公开(公告)号：NZ566068A
公开(公告)日：2011-03-31
申请号：NZ56606806
申请日：2006-08-08
申请人： ARGENTA DISCOVERY LTD
发明人： RAY NICHOLAS CHARLES , BULL RICHARD JAMES , FINCH HARRY , VAN NIEL MONIQUE BODIL , JENNINGS ANDREW STEPHEN ROBERT
IPC分类号： A61K31/221 , A61K31/27 , A61K31/352 , A61K31/381 , A61K31/451 , A61K31/4704 , A61P29/00 , C07C219/24 , C07C233/41 , C07C271/38 , C07D211/14 , C07D311/84 , C07D311/86 , C07D333/16 , C07D409/14
摘要： Disclosed is a bicyclo[2.2.1]hept-7-ylamine derivative of formula (I), wherein A is -O- or -N(R12)- and the other substituents are as defined in the specification. Also discloses is the use of the compound for treating a disease or condition in which M3 muscarinic receptor activity is implicated, such as a respiratory-tract disorder, a gastrointestinal-tract disorder, a cardiovascular disorder, chronic obstructive lung disease, chronic bronchitis, asthma, chronic respiratory obstruction, bronchial hyperactivity, pulmonary fibrosis, pulmonary emphysema, allergic rhinitis, irritable bowel syndrome, spasmodic colitis, gastroduodenal ulcers, gastrointestinal convulsions or hyperanakinesia, diverticulitis, pain accompanying spasms of gastrointestinal smooth musculature, urinary-tract disorders accompanying micturition disorders including neurogenic pollakiuria, neurogenic bladder, nocturnal enuresis, psychosomatic bladder, incontinence associated with bladder spasms or chronic cystitis, urinary urgency or pollakiuria, motion sickness, or cardiovascular disorders such as vagally induced sinus bradycardia.

9. 发明专利

BRPI0614290A2 未知
公开(公告)号：BRPI0614290A2
公开(公告)日：2011-03-22
申请号：BRPI0614290
申请日：2006-08-08
申请人： ARGENTA DISCOVERY LTD
发明人： RAY NICHOLAS CHARLES , BULL RICHARD JAMES , VAN NEIL MONIQUE BODIL , JENNINGS ANDREW STEPHEN ROBERT , FINCH HARRY
IPC分类号： C07C271/38 , A61K31/27 , A61K31/381 , A61K31/451 , C07C219/24 , C07C233/41 , C07D211/14 , C07D311/84 , C07D311/86 , C07D333/16 , C07D409/14
摘要： Compounds of formula (I) have muscarinic M3 receptor modulating activity; 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 -alkyl 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.

10. 发明专利

CO6190612A2 DERIVADOS HETEROCICLICOS COMO RECEPTORES MUSCARINICOS M3 未知
公开(公告)号：CO6190612A2
公开(公告)日：2010-08-19
申请号：CO09078490
申请日：2009-07-28
申请人： ARGENTA DISCOVERY LTD
发明人： AVITABILE BARBARA , FINCH HARRY , KNIGHT JAIME , NADIN ALAN , RAY NICHOLAS CHARLES
IPC分类号： C07D471/08
摘要： 1.- Un compuesto de la fórmula (I):dondeR2 es un grupo H -(Z)p-R7, -Z-Y-R7 o -Y-R7;p es 0 ó 1;R4 y R5 son independientemente seleccionados del grupo que consiste en aril, heterocicloalquil fusionado con aril, heteroaril, C1-C6-alquil y cicloalquil; R6 es -OH, C1-C6-alquil, C1-C6-alcoxi, hidroxi-C1-C6-alquil, nitrilo, un grupo CONR1R9 o un átomo de hidrógeno; uno de W, V y A es N o NR11; otro de W, V y A es N, O, S o CR8; y el último de W, V y A es N o CR8;X es un grupo C1-C4-alquileno, C2-C4-alquenileno o C2-C4-alquinileno; R7 es un grupo C1-C6-alquil, C2-C6-alquenil, aril, cicloalquil fusionado con aril, heterocicloalquil fusionado con aril, heteroaril, aril(C1-C8-alquil)-, heteroaril(C1-C8-alquil)-, heterocicloalquil o cicloalquil; t, u y v son independientemente seleccionados de 1, 2 ó 3, con la condición de que t, u y v no puedan todos ser simultáneamente 1; Z es un grupo C1-C4-alquileno, C2-C4-alquenileno o C2-C4-alquinileno; Y es un átomo de oxígeno, un grupo -OC(O)-, un grupo -N(H)C(O)- o un grupo -S(O)n;n es 0, 1 ó 2; R1, R8, R9 y R11 son, independientemente, un átomo de hidrógeno o un grupo C1-C6-alquil; y D- es un contraión farmacéuticamente aceptable; donde, a menos que se indique lo contrario, cada aparición de alquil, alquenil, heterocicloalquil, aril, heterocicloalquil fusionado con aril, heteroaril, cicloalquil, alcoxi, alquileno, alquenileno, alquinileno o cicloalquil fusionado con aril puede ser opcionalmente sustituida; y donde cada cadena de alquenileno contiene, donde sea posible, hasta 2 enlaces dobles carbono-carbono y cada cadena de alquinileno contiene, donde sea posible, hasta 2 enlaces triples carbono-carbono.

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