公开(公告)号：US20060111344A1

公开(公告)日：2006-05-25

申请号：US10522321

申请日：2003-07-24

申请人： Keith Biggadike ,  Diane Coe ,  Duncan Holmes ,  Brian Looker

发明人： Keith Biggadike ,  Diane Coe ,  Duncan Holmes ,  Brian Looker

IPC分类号： A61K31/549 ,  A61K31/538 ,  A61K31/4704 ,  A61K31/405 ,  A61K31/428 ,  A61K31/325 ,  A61K31/138 ,  A61K31/165

CPC分类号： C07D277/68 ,  C07C311/29 ,  C07D213/65 ,  C07D215/26 ,  C07D265/36

摘要： The present invention relates to compounds of formula (I) as defined herein and salts or solvates thereof. Processes for preparing these compounds and pharmaceutical formulations containing them are also disclosed, as well as methods for the prophylaxis of treatment of a clinical condition using such compounds.

摘要翻译： 本发明涉及本文定义的式（I）化合物及其盐或溶剂化物。 还公开了制备这些化合物的方法和含有它们的药物制剂的方法，以及用于预防使用这些化合物治疗临床病症的方法。

公开(公告)号：US06878698B2

公开(公告)日：2005-04-12

申请号：US10281735

申请日：2002-10-28

申请人： Keith Biggadike ,  Paul Spencer Jones ,  Jeremy John Payne

发明人： Keith Biggadike ,  Paul Spencer Jones ,  Jeremy John Payne

IPC分类号： A61K9/00 ,  A61K9/14 ,  A61K31/18 ,  A61K31/573 ,  A61K31/58 ,  A61K45/06 ,  A61L9/04 ,  C07J17/00 ,  C07J31/00 ,  C07J33/00 ,  C07J43/00

CPC分类号： A61K9/0075 ,  A61K9/008 ,  A61K31/18 ,  A61K31/573 ,  A61K31/58 ,  A61K45/06 ,  C07J17/00 ,  C07J31/00 ,  C07J33/002 ,  C07J43/003 ,  A61K2300/00

摘要： According to one aspect of the invention, there is provided a pharmaceutical formulation for administration by inhalation comprising a compound of formula (I), wherein R1 represents C1-6 alkyl or C1-6 haloalkyl; R2 represents —C(═O)-aryl or —C(═O)-heteroaryl; R3 represents hydrogen, methyl (which may be in either the α or β configuration) or methylene; R4 and R5 are the same or different and each represents hydrogen or halogen; and represents a single or a double bond; and salts and solvates thereof together with a long-acting β2-adrenoreceptor agonist which formulation has a therapeutically useful effect in the treatment of COPD over a period of 24 hours or more.

摘要翻译： 根据本发明的一个方面，提供了一种用于通过吸入给药的药物制剂，其包含式（I）化合物，其中R 1表示C 1-6烷基或C 1-6卤代烷基; R 2表示-C（= O） - 芳基或 -C（= O） - 杂芳基; R 3表示氢，甲基（其可以是α或β构型）或亚甲基; R 4和R 5相同或不同，各自表示氢或卤素; 和表示单键或双键 ;以及其与长效β2-肾上腺素受体激动剂的盐和溶剂化物，该制剂在24小时或更长时间内治疗COPD具有治疗上有效的作用。

公开(公告)号：US20050070515A1

公开(公告)日：2005-03-31

申请号：US10635680

申请日：2003-08-07

申请人： Richard Angell ,  Keith Biggadike ,  Rosanne Farrell ,  Duncan Holmes ,  Panayiotis Procopiou

发明人： Richard Angell ,  Keith Biggadike ,  Rosanne Farrell ,  Duncan Holmes ,  Panayiotis Procopiou

IPC分类号： C07J3/00 ,  C07J17/00 ,  C07J31/00 ,  C07J33/00 ,  C07J71/00 ,  C12Q1/44 ,  A61K31/58 ,  A61K31/585

CPC分类号： C07J17/00 ,  C07J3/005 ,  C07J31/006 ,  C07J33/005 ,  C07J71/0031 ,  C12Q1/44 ,  G01N2333/918 ,  G01N2500/00

摘要： Compounds capable of providing a therapeutic effect at a target site within a human or animal body with reduced systemic potency to said body are identified by comparing the susceptibility to hydrolysis of the compound in the presence of a purified lactonase enzyme or a recombinant form of it to the corresponding susceptibility in the absence of said lactonase enzyme, and then selecting a compound on the basis of enhanced susceptibility to hydrolysis in the presence of said lactonase enzyme

摘要翻译： 通过比较在纯化的内含酶或其重组形式的存在下化合物的水解易感性，通过比较在所述身体中的纯化内酯酶或其重组形式的存在下对水解的易感性，其能够在人或动物体内的靶位点提供治疗效果， 在不存在所述内含酶的情况下相应的易感性，然后在所述内含酶存在下，基于增加的水解易感性选择化合物

公开(公告)号：US06777399B2

公开(公告)日：2004-08-17

申请号：US10067010

申请日：2002-02-04

申请人： Keith Biggadike ,  Steven John Coote ,  Andrew S. Craig ,  Victor W Jacewicz ,  Michael J. Millan ,  Rosalyn K. Nice ,  Brian M Noga ,  John F. Seager ,  Andrew L. Theophilus ,  David M. Crowe

发明人： Keith Biggadike ,  Steven John Coote ,  Andrew S. Craig ,  Victor W Jacewicz ,  Michael J. Millan ,  Rosalyn K. Nice ,  Brian M Noga ,  John F. Seager ,  Andrew L. Theophilus ,  David M. Crowe

IPC分类号： A61K3158

CPC分类号： C07J31/00 ,  C07J17/00

摘要： There is provided a crystalline chemical composition comprising a compound of formula (I) in which the crystal lattice is stabilized by the presence of a guest molecule, characterized in the crystalline composition is of space group P212121 having unit cell dimensions of about 12.1±0.6 Å, 14.9±0.7 Å, and 16.2±0.8 Å when determined at either 120K or 150K.

摘要翻译： 提供了包含式（I）化合物的结晶化学组合物，其中通过客体分子的存在使晶格稳定，其特征在于晶体组成为具有约12.1±0.6的晶胞尺寸的空间群P212121 ，14.9±0.7Å和16.2±0.8Å，当在120K或150K下测定时。

公开(公告)号：US5100896A

公开(公告)日：1992-03-31

申请号：US556262

申请日：1990-07-23

申请人： Alan D. Borthwick ,  Keith Biggadike ,  Barrie E. Kirk ,  Richard Storer ,  Niall G. Weir ,  Anthony D. Baxter ,  Chi L. Mo

发明人： Alan D. Borthwick ,  Keith Biggadike ,  Barrie E. Kirk ,  Richard Storer ,  Niall G. Weir ,  Anthony D. Baxter ,  Chi L. Mo

IPC分类号： A61K31/505 ,  A61P31/12 ,  C07D487/04

CPC分类号： C07D487/04

摘要： The present invention provides a compound of formula (I) ##STR1## and salts and solvates and pharmaceutically acceptable derivatives thereof, and describes processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of viral diseases, especially those caused by the Herpetoviridae.

公开(公告)号：US08178573B2

公开(公告)日：2012-05-15

申请号：US12226372

申请日：2007-04-18

申请人： Keith Biggadike ,  Anthony William James Cooper ,  David House ,  Iain McFarlane McLay ,  Grahame Robert Woollam

发明人： Keith Biggadike ,  Anthony William James Cooper ,  David House ,  Iain McFarlane McLay ,  Grahame Robert Woollam

IPC分类号： A61K31/416 ,  C07D231/56

CPC分类号： C07D403/10 ,  C07D231/56

摘要： The present invention provides compounds of formula (I): pharmaceutical compositions comprising the compounds and the use of the compounds for the manufacture of a medicament, particularly for the treatment of inflammation and/or allergic conditions.

摘要翻译： 本发明提供式（I）化合物：包含该化合物的药物组合物和该化合物在制备药物中的用途，特别是用于治疗炎症和/或过敏性疾病。

公开(公告)号：US20100120883A1

公开(公告)日：2010-05-13

申请号：US12444713

申请日：2007-10-10

申请人： Keith Biggadike ,  Anthony William James Cooper ,  David House ,  Simon John Fawcett MacDonald ,  Philip Alan Skone ,  Gordon Gad Weingarten

发明人： Keith Biggadike ,  Anthony William James Cooper ,  David House ,  Simon John Fawcett MacDonald ,  Philip Alan Skone ,  Gordon Gad Weingarten

IPC分类号： A61K31/416 ,  C07D231/56 ,  C07D409/12 ,  A61P11/02 ,  A61P11/00 ,  A61P27/14 ,  A61P11/06 ,  A61P29/00 ,  A61P5/44 ,  A61P17/00 ,  A61P17/06

CPC分类号： C07D231/56 ,  C07C251/86 ,  C07D405/12 ,  C07D409/12 ,  Y10S514/885

摘要： The present invention provides compounds of formula (I): a process for their preparation, pharmaceutical compositions comprising the compounds and the preparation of said compositions, intermediates and use of the compounds for the manufacture of a medicament for therapeutic treatment, particularly for the treatment of inflammation, allergy and/or skin disease.

摘要翻译： 本发明提供式（I）化合物：其制备方法，包含所述化合物的药物组合物和所述组合物的制备，所述化合物的中间体和用途，用于制备用于治疗性治疗的药物，特别是用于治疗 炎症，过敏和/或皮肤疾病。

公开(公告)号：US20100075995A1

公开(公告)日：2010-03-25

申请号：US12537392

申请日：2009-08-07

申请人： Keith Biggadike ,  Diane Mary Coe ,  Xiao Qing Lewell ,  Charlotte Jane Mitchell ,  Stephen Allan Smith ,  Naimisha Trivedi

发明人： Keith Biggadike ,  Diane Mary Coe ,  Xiao Qing Lewell ,  Charlotte Jane Mitchell ,  Stephen Allan Smith ,  Naimisha Trivedi

IPC分类号： A61K31/522 ,  C07D473/18 ,  A61P11/06

CPC分类号： A61K31/522 ,  A61K9/0043 ,  A61K31/55 ,  A61K45/06 ,  A61P29/00 ,  A61P31/00 ,  A61P35/00 ,  A61P37/00 ,  C07D473/16 ,  C07D473/18

摘要： Compounds of formula (I): wherein R1 is C1-6alkylamino, C1-6alkoxy, or C3-7cycloalkyloxy; m is an integer having a value of 3 to 6; n is an integer having a value of 0 to 4; and salts thereof are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, the treatment of infectious diseases and cancer, and may also be useful as vaccine adjuvants.

摘要翻译： 式（I）化合物：其中R 1是C 1-6烷基氨基，C 1-6烷氧基或C 3-7环烷氧基; m为3〜6的整数， n为0〜4的整数， 其盐是人类干扰素的诱导剂。 诱导人类干扰素的化合物可用于治疗各种疾病，例如治疗过敏性疾病和其它炎性病症，例如过敏性鼻炎和哮喘，治疗感染性疾病和癌症，并且也可用作疫苗佐剂。

公开(公告)号：US07592329B2

公开(公告)日：2009-09-22

申请号：US10503114

申请日：2003-02-04

申请人： Keith Biggadike ,  Steven John Coote ,  Andrew Craig ,  David Malcolm Crowe ,  Victor Witold Jacewicz ,  Michael John Millan ,  Rosalyn Kay Nice ,  Brian Noga ,  John Frederick Seager ,  Andrew Lewis Theophilus

发明人： Keith Biggadike ,  Steven John Coote ,  Andrew Craig ,  David Malcolm Crowe ,  Victor Witold Jacewicz ,  Michael John Millan ,  Rosalyn Kay Nice ,  Brian Noga ,  John Frederick Seager ,  Andrew Lewis Theophilus

IPC分类号： A61K31/58 ,  C07J17/00

CPC分类号： C07J31/00 ,  C07J17/00

摘要： There is provided a crystalline complex comprising a compound of formula (I) in which the crystal lattice is stabilized by the presence of a guest molecule, characterized in that the crystalline complex is of space group P212121 having unit cell dimensions of about 12.5±1.0 §, 15±1.0 §, and 16.2±1.0 § when determined at either 120K or 150K.

摘要翻译： 提供了一种结晶复合物，其包含式（I）化合物，其中晶格通过客体分子的存在而稳定，其特征在于结晶复合物为具有约12.5±1.0的晶胞尺寸的空间群P212121§ ，15±1.0§和16.2±1.0§当在120K或150K下测定时。

公开(公告)号：US07579335B2

公开(公告)日：2009-08-25

申请号：US11813227

申请日：2006-01-09

申请人： Keith Biggadike ,  Deborah Needham

发明人： Keith Biggadike ,  Deborah Needham

IPC分类号： A61K31/56 ,  C07J3/00

CPC分类号： C07J3/005 ,  C07J41/0094

摘要： The present invention is directed to compounds of formula (I): wherein R1 represents C4-C7 branched alkyl group, a bicycloalkyl group, or a C5-C6 cycloalkyl which optionally may be substituted with a C1-C4 alkyl group; R2 represents hydrogen, a methyl group, which may be in either the α or β configuration, or a methylene group; R3 and R4 are the same or a different group and each independently represents hydrogen, halogen or a methyl group; represents a single or a double bond; and physiologically acceptable solvates thereof, physiologically functional derivatives thereof, pharmaceutical compositions comprising the compounds, the use of the compounds for the manufacture of medicaments particularly for the treatment of inflammatory and/or allergic conditions, processes for the preparation of the compounds, and chemical intermediates in the processes for the manufacture of the compounds.

摘要翻译： 本发明涉及式（I）的化合物：其中R1表示C4-C7支链烷基，双环烷基或任选可被C 1 -C 4烷基取代的C 5 -C 6环烷基; R 2表示氢，可以是α或β构型的甲基或亚甲基; R3和R4相同或不同，各自独立地表示氢，卤素或甲基; “img id =”CUSTOM-CHARACTER-00001“he =”2.79mm“wi =”4.23mm“file =”US07579335-20090825-P00001.TIF“alt =”custom character“img-content =”character“img-format =“tif”/>表示单键或双键; 及其生理学上可接受的溶剂合物，其生理功能衍生物，包含该化合物的药物组合物，用于制备药物，特别是用于治疗炎症和/或过敏病症的化合物的用途，用于制备化合物的方法和化学中间体 在制备化合物的方法中。