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11.
公开(公告)号:US20090238808A1
公开(公告)日:2009-09-24
申请号:US12002222
申请日:2007-12-14
申请人: Gerard Drewes , Bernhard Kuester , Ulrich Kruse , Carsten Hopf , Dirk Eberhard , Marcus Bantscheff , Valerie Reader , Manfred Raida , David Middlemiss
发明人: Gerard Drewes , Bernhard Kuester , Ulrich Kruse , Carsten Hopf , Dirk Eberhard , Marcus Bantscheff , Valerie Reader , Manfred Raida , David Middlemiss
IPC分类号: A61K38/43 , G01N33/573
CPC分类号: G01N33/6848 , C12Q1/485
摘要: The present invention relates to methods for the characterization of enzymes or of enzyme-compound complexes, wherein the enzyme is obtained from a protein preparation with the help of at least one broad spectrum ligand immobilized on a solid support and wherein the enzyme is characterized by mass spectrometry. These methods are useful for the screening of non-immobilized compound libraries, selectivity profiling of lead compounds and mechanism of action studies in living cells.
摘要翻译: 本发明涉及用于表征酶或酶 - 化合物复合物的方法,其中所述酶是借助于固定在固体支持物上的至少一个宽谱图配体从蛋白质制备物获得的,其中所述酶的特征在于质量 光谱测定。 这些方法可用于非固定化化合物文库的筛选,铅化合物的选择性分析以及活细胞的作用机制研究。
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公开(公告)号:US20080234292A1
公开(公告)日:2008-09-25
申请号:US11571857
申请日:2005-07-21
申请人: Susan Marie Royalty , James Ford Burns , Jan Jozef Scicinski , Gunnar Erik Jagdmann, Jr. , Robert James Foglesong , Kellee Griffin Ring , Tatyana Dyakonov , David Middlemiss
发明人: Susan Marie Royalty , James Ford Burns , Jan Jozef Scicinski , Gunnar Erik Jagdmann, Jr. , Robert James Foglesong , Kellee Griffin Ring , Tatyana Dyakonov , David Middlemiss
IPC分类号: A61K31/40 , C07D207/16 , C07D401/12 , C07D403/12 , C07D413/12 , C07D277/04 , A61K31/497 , A61K31/506 , A61K31/4439 , A61K31/426 , A61K31/422 , A61P3/10
CPC分类号: C07D207/10 , C07D207/16 , C07D277/04 , C07D401/12 , C07D403/12 , C07D405/12
摘要: The present invention relates to a series of novel compounds having the formula (I) wherein: X is NR3 or O; n is 1 or 2; A is a bicyclic carbocycle and R1 and R2 are as described herein. The compounds are useful as DPP-IV inhibitors, such as for the treatment of diabetes.
摘要翻译: 本发明涉及一系列具有式(I)的新化合物,其中:X为NR 3或O; n为1或2; A是双环碳环,R 1和R 2如本文所述。 该化合物可用作DPP-IV抑制剂,例如治疗糖尿病。
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公开(公告)号:US20070232681A1
公开(公告)日:2007-10-04
申请号:US10573670
申请日:2004-10-13
申请人: David Middlemiss , Mark Ashton , Edward Boyd , Frederick Brookfield , Richard Armer , Eric Pettipher
发明人: David Middlemiss , Mark Ashton , Edward Boyd , Frederick Brookfield , Richard Armer , Eric Pettipher
IPC分类号: A61K31/40 , A61K31/405 , C07D209/04 , C07D209/34
CPC分类号: C04B35/632 , C07D209/30 , C07D401/12 , C07D403/12 , C07D417/12
摘要: Compounds of general formula (I): wherein R1, R2, R3 and R4 are independently hydrogen, halo, C1-C6 alkyl, —O(C1-C6 alkyl), —CON(R9)2, —SOR9, —SO2R9, —SO2N(R9)2, —N(R9)2, —NR9COR9, —CO2R9, —COR9, —SR9, —OH, —NO2 or —CN; each R9 is independently hydrogen or C1-C6 alkyl; R5 and R6 are each independently hydrogen, or C1-C6 alkyl or together with the carbon atom to which they are attached form a C3-C7 cycloalkyl group; R7 is hydrogen or C1-C6 alkyl n is 1 or 2; X is a bond or, when n is 2, X may also be a NR9 group; wherein R9 is as defined above; when X is a bond R8 is C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, biphenyl or a 9-14 membered bicyclic or tricyclic heteroaryl group; when X is a NR9 group R8 may additionally be phenyl, naphthyl or a 5-7 membered heteroaromatic ring; and the R8 group is optionally substituted with one or more substituents selected from halo, C1-C6 alkyl, —O(C1-C6)alkyl, aryl, —O-aryl, heteroaryl, —O-heteroaryl, —CON(R9)2, —SOR9, —SO2R9, SO2N(9)2, —N(9)2, —NR9COR9, —CO2R9, —COR9, —SR9, —OH, —NO2 or —CN; wherein R9 is as defined above; and their pharmaceutically acceptable salts, hydrates, solvates, complexes and prodrugs are useful in the treatment of allergic diseases such as asthma, allergic rhinitis and atopic dermatitis.
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公开(公告)号:US20050119268A1
公开(公告)日:2005-06-02
申请号:US10972060
申请日:2004-10-22
IPC分类号: A61K31/404 , A61K31/426 , A61K31/428 , A61K31/4709 , A61K31/498 , C07D209/08 , C07D209/10 , C07D209/12 , C07D401/06 , C07D403/06 , C07D417/06 , A61K31/405 , A61K31/427 , C07D417/02 , C07D43/02
CPC分类号: C07D209/12 , A61K31/404 , A61K31/426 , A61K31/428 , A61K31/4709 , A61K31/498 , C07D209/08 , C07D209/10 , C07D401/06 , C07D403/06 , C07D417/06
摘要: The present invention provides indole derivatives that antagonize prostaglandin D2, and that can be used to treat inflammatory diseases mediated by prostaglandin D2.
摘要翻译: 本发明提供了拮抗前列腺素D 2 N的吲哚衍生物,其可用于治疗由前列腺素D 2 2介导的炎性疾病。
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公开(公告)号:US5703240A
公开(公告)日:1997-12-30
申请号:US612843
申请日:1996-03-21
申请人: Duncan Robert Armour , Brian Evans , David Middlemiss , Alan Naylor , Neil Anthony Pegg , Maria Victoria Vinader , Gerard Martin Paul Giblin , Tania Hubbard , Michael Menteith Hann , Xiao-Qing Lewell , Stephen Paul Watson
发明人: Duncan Robert Armour , Brian Evans , David Middlemiss , Alan Naylor , Neil Anthony Pegg , Maria Victoria Vinader , Gerard Martin Paul Giblin , Tania Hubbard , Michael Menteith Hann , Xiao-Qing Lewell , Stephen Paul Watson
IPC分类号: A61K31/44 , A61K31/4427 , A61K31/445 , A61K31/4523 , A61K31/454 , A61P1/00 , A61P1/08 , A61P25/04 , A61P29/00 , A61P43/00 , C07D20060101 , C07D211/56 , C07D401/10 , C07D401/12
CPC分类号: C07D401/12
摘要: The present invention relates to piperidine derivatives of formula (I) ##STR1## wherein R.sup.1 is a C.sub.1-4 alkoxy group; R.sup.2 is ##STR2## R.sup.3 is a hydrogen or halogen atom; R.sup.4 and R.sup.5 may each independently represent a hydrogen or halogen atom, or a C.sub.1-4 alkyl, C.sub.1-4 alkoxy or trifluoromethyl group; R.sup.6 is a hydrogen atom, a C.sub.1-4 alkyl, (CH.sub.2).sub.m cyclopropyl, --S(O).sub.n C.sub.1-4 alkyl, phenyl, NR.sup.7 R.sup.8, CH.sub.2 C(O)CF.sub.3 or trifluoromethyl group; R.sup.7 and R.sup.8 may each independently represent a hydrogen atom, or a C.sub.1-4 alkyl or acyl group; x represents zero or 1; n represents zero, 1 or 2; m represents zero or 1; and pharmaceutically acceptable salts and solvates thereof; to processes for their preparation; and their use in the treatment of conditions mediated by tachykinins.
摘要翻译: PCT No.PCT / EP94 / 03129 Sec。 371日期1996年3月21日 102(e)1996年3月21日PCT PCT 1994年9月20日PCT公布。 第WO95 / 08549号公报 日期:1995年3月30日本发明涉及式(I)的哌啶衍生物其中R 1为C 1-4烷氧基; R 2是氢或卤素原子; R 4和R 5可各自独立地表示氢或卤素原子,或C 1-4烷基,C 1-4烷氧基或三氟甲基; R6是氢原子,C1-4烷基,(CH2)环丙基,-S(O)nC1-4烷基,苯基,NR7R8,CH2C(O)CF3或三氟甲基; R 7和R 8可各自独立地表示氢原子或C 1-4烷基或酰基; x表示零或1; n表示0,1或2; m表示0或1; 及其药学上可接受的盐和溶剂合物; 进行准备; 及其用于治疗由速激肽介导的病症。
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公开(公告)号:US5317023A
公开(公告)日:1994-05-31
申请号:US883386
申请日:1992-05-15
申请人: Barry C. Ross , David Middlemiss , David I. C. Scopes , Torquil I. M. Jack , Kevin S. Cardwell , Michael D. Dowle , John G. Montana , Martin Pass , Duncan B. Judd
发明人: Barry C. Ross , David Middlemiss , David I. C. Scopes , Torquil I. M. Jack , Kevin S. Cardwell , Michael D. Dowle , John G. Montana , Martin Pass , Duncan B. Judd
IPC分类号: A61K31/435 , A61K31/50 , A61K31/505 , A61K31/52 , A61P3/08 , A61P9/00 , A61P9/12 , A61P25/28 , A61P43/00 , C07D405/06 , C07D405/14 , C07D471/04 , C07D473/00 , C07D473/40 , C07D487/04 , C07D401/048 , A61K31/44
CPC分类号: C07D405/14 , C07D471/04 , C07D473/00
摘要: The invention provides compounds of formula (I): ##STR1## or a physiologically acceptable salt, solvate or metabolically labile ester thereof whereinR.sup.1 represents a hydrogen atom or a halogen atom or a group selected from C.sub.1-6 alkyl, C.sub.2-6 alkenyl, fluoroC.sub.1-6 alkyl, C.sub.1-6 alkoxy, --CHO, --CO.sub.2 H or --COR.sup.2 ;Ar represents optionally substituted phenylHet represents the group ##STR2## A represents ##STR3## The compounds may be used in the treatment or prophylaxis of hypertension and diseases associated with cognitive disorders.
摘要翻译: 本发明提供式(I)化合物:其溶剂合物或代谢不稳定的酯,其中R 1表示氢原子或卤素原子或选自C 1-6烷基,C 2-6烯基,氟C 1-6烷基,C 1-6烷氧基, CHO,-CO 2 H或-COR 2; Ar表示任选取代的苯基Het表示基团A表示高血压和与认知障碍相关的疾病的预防或预防。
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公开(公告)号:US4908386A
公开(公告)日:1990-03-13
申请号:US287441
申请日:1988-12-20
申请人: Harry Finch , Lawrence H. C. Lunts , Alan Naylor , Ian F. Skidmore , Ian B. Campbell , David Middlemiss , Charles Willbe
发明人: Harry Finch , Lawrence H. C. Lunts , Alan Naylor , Ian F. Skidmore , Ian B. Campbell , David Middlemiss , Charles Willbe
IPC分类号: C07D213/65 , C07D295/096 , C07C143/74 , A61K31/18
CPC分类号: C07D295/096 , C07D213/65 , Y10S514/826
摘要: The present invention provides compounds of general formula (I) ##STR1## wherein Ar represents an unsubstituted or substituted phenyl gorup;R.sup.1 and R.sup.2 each represents a hydrogen atom or a C.sub.1-3 alkyl group;X represents a bond or a C.sub.1-7 alkylene, C.sub.2-7 alkenylene or C.sub.2-7 alkynylene chain;Y represents a bond or a C.sub.1-6 alkylene, C.sub.2-6 alkenylene or C.sub.2-6 alkynylene chain;Q represents a substituted phenyl or pyridyl ring;and physiologically acceptable salts and solvates thereof useful as stimulants of .sub.2 -adrenoreceptors and particularly in the treatment of diseases associated with reversible airways obstruction such as asthma and chronic bronchitis.
摘要翻译: 本发明提供通式(I)的化合物,其中Ar表示未取代或取代的苯基; R1和R2各自表示氢原子或C1-3烷基; X表示键或C 1-7亚烷基,C 2-7亚烯基或C 2-7亚炔基链; Y表示键或C 1-6亚烷基,C 2-6亚烯基或C 2-6亚炔基链; Q表示取代的苯基或吡啶环; 以及其可用作2-肾上腺素受体的兴奋剂的生理上可接受的盐和溶剂合物,特别是用于治疗与可逆气道阻塞如哮喘和慢性支气管炎相关的疾病。
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公开(公告)号:US08163936B2
公开(公告)日:2012-04-24
申请号:US12232445
申请日:2008-09-17
申请人: David Middlemiss , Mark Richard Ashton , Edward Andrew Boyd , Frederick Arthur Brookfield , Michael George Hunter , Mark Whittaker , Chris Palmer , Eric R. Pettipher
发明人: David Middlemiss , Mark Richard Ashton , Edward Andrew Boyd , Frederick Arthur Brookfield , Michael George Hunter , Mark Whittaker , Chris Palmer , Eric R. Pettipher
IPC分类号: C07D215/38
CPC分类号: C07D209/12 , A61K31/404 , A61K31/426 , A61K31/428 , A61K31/4709 , A61K31/498 , C07D209/08 , C07D209/10 , C07D401/06 , C07D403/06 , C07D417/06
摘要: The present invention provides indole derivatives that antagonize prostaglandin D2, and that can be used to treat inflammatory diseases mediated by prostaglandin D2.
摘要翻译: 本发明提供了拮抗前列腺素D2的吲哚衍生物,其可用于治疗由前列腺素D2介导的炎性疾病。
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公开(公告)号:US07842707B2
公开(公告)日:2010-11-30
申请号:US11571857
申请日:2005-07-21
申请人: Susan Marie Royalty , James Ford Burns , Jan Jozef Scicinski , Gunnar Erik Jagdmann, Jr. , Robert James Foglesong , Kellee Griffin Ring , Tatyana Dyakonov , David Middlemiss
发明人: Susan Marie Royalty , James Ford Burns , Jan Jozef Scicinski , Gunnar Erik Jagdmann, Jr. , Robert James Foglesong , Kellee Griffin Ring , Tatyana Dyakonov , David Middlemiss
IPC分类号: A01N43/40 , A01N43/78 , A01N43/80 , A01N43/36 , A61K31/44 , A61K31/425 , A61K31/42 , A61K31/40 , C07D401/00 , C07D277/00 , C07D261/00 , C07D295/00
CPC分类号: C07D207/10 , C07D207/16 , C07D277/04 , C07D401/12 , C07D403/12 , C07D405/12
摘要: The present invention relates to a series of novel compounds having the formula (I) wherein: X is NR3 or O; n is 1 or 2; A is a bicyclic carbocycle and R1 and R2 are as described herein. The compounds are useful as DPP-IV inhibitors, such as for the treatment of diabetes.
摘要翻译: 本发明涉及一系列具有式(I)的新化合物,其中:X为NR 3或O; n为1或2; A是双环碳环,R 1和R 2如本文所述。 该化合物可用作DPP-IV抑制剂,例如治疗糖尿病。
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20.
公开(公告)号:US20100137300A1
公开(公告)日:2010-06-03
申请号:US12530929
申请日:2007-03-21
申请人: George Hynd , Nicholas Charles Ray , Harry Finch , John Gary Montana , Michael Colin Cramp , Trevor Keith Harrison , Rosa Arienzo , Paul Blaney , Yann Griffon , David Middlemiss
发明人: George Hynd , Nicholas Charles Ray , Harry Finch , John Gary Montana , Michael Colin Cramp , Trevor Keith Harrison , Rosa Arienzo , Paul Blaney , Yann Griffon , David Middlemiss
IPC分类号: A61K31/5377 , A61K31/435 , A61K31/4709 , C07D413/12 , C07D221/04 , C07D215/14 , A61P1/00 , A61P11/06 , A61P11/00 , A61P1/04
CPC分类号: 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.
摘要翻译: 该列表的具体化合物:{7-氰基-2-甲基-1- [4-(吗啉-4-磺酰基)苄基]中氮茚-3-基}乙酸,{1-(3-氯-4-乙磺酰基苄基 )-7-氰基-2-甲基吲哚啉-3-基}乙酸{1- [3-氯-4-(吗啉-4-磺酰基)苄基] -7-氰基-2-甲基吲哚啉-3-基}乙酸, {1-(3-氯-4-乙磺酰基苯基硫烷基)-7-氰基-2-甲基吲哚啉-3-基}乙酸{1- [3-氯-4-(吗啉-4-磺基)苯基f烷基] 氰基-2-甲基吲哚啉-3-基}乙酸,{7-氰基-1-(6-氟喹啉-2-基甲基)-2-甲基吲哚啉-3-基}乙酸是CRTH2受体的配体,可用于 治疗呼吸系统疾病。
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