公开(公告)号：US07442837B2

公开(公告)日：2008-10-28

申请号：US11426661

申请日：2006-06-27

申请人： Keith Biggadike ,  Diane Mary Coe ,  Dean David Edney ,  Stephen Barry Guntrip ,  Abigail Halton ,  Brian Edgar Looker ,  Michael John Monteith ,  Rebecca Jane Moore ,  Rajnikant Patel ,  Panayiotis Alexandrou Procopiou

发明人： Keith Biggadike ,  Diane Mary Coe ,  Dean David Edney ,  Stephen Barry Guntrip ,  Abigail Halton ,  Brian Edgar Looker ,  Michael John Monteith ,  Rebecca Jane Moore ,  Rajnikant Patel ,  Panayiotis Alexandrou Procopiou

IPC分类号： C07C303/00

CPC分类号： C07D295/26 ,  C07C311/27 ,  C07C311/29 ,  C07C311/58 ,  C07C2601/04 ,  C07C2601/14 ,  C07D295/13

摘要： The present invention relates to novel compounds of Formula (I), to a process for their manufacture, to pharmaceutical compositions containing them, and to their use in therapy, in particular their use in the prophylaxis and treatment of respiratory diseases.

公开(公告)号：US07442719B2

公开(公告)日：2008-10-28

申请号：US11207967

申请日：2005-08-19

申请人： Keith Biggadike ,  Diane Mary Coe ,  Dean David Edney ,  Stephen Barry Guntrip ,  Abigail Halton ,  Brian Edgar Looker ,  Michael John Monteith ,  Rebecca Jane Moore ,  Rajnikant Patel ,  Panayiotis Alexandrou Procopiou

发明人： Keith Biggadike ,  Diane Mary Coe ,  Dean David Edney ,  Stephen Barry Guntrip ,  Abigail Halton ,  Brian Edgar Looker ,  Michael John Monteith ,  Rebecca Jane Moore ,  Rajnikant Patel ,  Panayiotis Alexandrou Procopiou

IPC分类号： A01N41/06

CPC分类号： C07D295/26 ,  C07C311/27 ,  C07C311/29 ,  C07C311/58 ,  C07C2601/04 ,  C07C2601/14 ,  C07D295/13

摘要： The present invention relates to novel compounds of Formula (I), to a process for their manufacture, to pharmaceutical compositions containing them, and to their use in therapy, in particular their use in the prophylaxis and treatment of respiratory diseases.

摘要翻译： 本发明涉及式（I）的新化合物，其制备方法，含有它们的药物组合物及其在治疗中的用途，特别是其在预防和治疗呼吸系统疾病中的用途。

公开(公告)号：US07442836B2

公开(公告)日：2008-10-28

申请号：US11426657

申请日：2006-06-27

申请人： Keith Biggadike ,  Diane Mary Coe ,  Dean David Edney ,  Stephen Barry Guntrip ,  Abigail Halton ,  Brian Edgar Looker ,  Michael John Monteith ,  Rebecca Jane Moore ,  Rajnikant Patel ,  Panayiotis Alexandrou Procopiou

发明人： Keith Biggadike ,  Diane Mary Coe ,  Dean David Edney ,  Stephen Barry Guntrip ,  Abigail Halton ,  Brian Edgar Looker ,  Michael John Monteith ,  Rebecca Jane Moore ,  Rajnikant Patel ,  Panayiotis Alexandrou Procopiou

IPC分类号： C07C303/00

CPC分类号： C07D295/26 ,  C07C311/27 ,  C07C311/29 ,  C07C311/58 ,  C07C2601/04 ,  C07C2601/14 ,  C07D295/13

摘要： The present invention relates to novel compounds of Formula (I), to a process for their manufacture, to pharmaceutical compositions containing them, and to their use in therapy, in particular their use in the prophylaxis and treatment of respiratory diseases.

摘要翻译： 本发明涉及式（I）的新化合物，其制备方法，含有它们的药物组合物及其在治疗中的用途，特别是其在预防和治疗呼吸系统疾病中的用途。

公开(公告)号：US07135600B2

公开(公告)日：2006-11-14

申请号：US10467733

申请日：2002-02-11

申请人： Keith Biggadike ,  Diane Mary Coe ,  Stephen Barry Guntrip ,  Brian Edgar Looker ,  Panayiotis Alexandrou Procopiou

发明人： Keith Biggadike ,  Diane Mary Coe ,  Stephen Barry Guntrip ,  Brian Edgar Looker ,  Panayiotis Alexandrou Procopiou

IPC分类号： C07C39/12

CPC分类号： C07D295/26 ,  C07C311/27 ,  C07C311/29 ,  C07C311/58 ,  C07C2601/04 ,  C07C2601/14 ,  C07D295/13

摘要： The present invention relates to novel compounds of Formula (I), to a process for their manufacture, to pharmaceutical compositions containing them, and to their use in therapy, in particular their use in the prophylaxis and treatment of respiratory diseases.

摘要翻译： 本发明涉及式（I）的新化合物，其制备方法，含有它们的药物组合物及其在治疗中的用途，特别是其在预防和治疗呼吸系统疾病中的用途。

公开(公告)号：US07538127B2

公开(公告)日：2009-05-26

申请号：US10544869

申请日：2004-02-12

申请人： Keith Biggadike ,  Philip Charles Box ,  Diane Mary Coe ,  Duncan Stuart Holmes ,  Brian Edgar Looker ,  Panayiotis Alexandrou Procopiou

发明人： Keith Biggadike ,  Philip Charles Box ,  Diane Mary Coe ,  Duncan Stuart Holmes ,  Brian Edgar Looker ,  Panayiotis Alexandrou Procopiou

IPC分类号： C07D213/65 ,  C07C217/08 ,  A61K31/44 ,  A61K31/18

CPC分类号： C07D213/65 ,  C07C217/28

摘要： A compound of formula (I) or a salt, solvate, or physiologically functional derivative thereof, wherein: m is an integer of from 2 to 8; n is an integer of from 2 to 5; with the proviso that m+n is 4 to 10; R4 and R5 are independently selected from hydrogen and C1-4alkyl with the proviso that the total number of carbon atoms in R4 and R5 not more than 4; R6 and R7 are independently selected from hydrogen and C1-4alkyl with the proviso that the total number of carbon atoms in R6 and R7 is not more than 4, and Ar1 is a group selected from (a), (b), (c) and (d).

摘要翻译： 式（I）化合物或其盐，溶剂合物或生理功能衍生物，其中：m为2至8的整数; n为2〜5的整数， 条件是m + n为4至10; R4和R5独立地选自氢和C1-4烷基，条件是R4和R5中的碳原子总数不大于4; R6和R7独立地选自氢和C1-4烷基，条件是R6和R7中的碳原子总数不大于4，Ar1是选自（a），（b），（c）中的基团， 和（d）。

公开(公告)号：US07402598B2

公开(公告)日：2008-07-22

申请号：US10522321

申请日：2003-07-24

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

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

IPC分类号： A61K31/47 ,  C07D215/22

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：US07045658B2

公开(公告)日：2006-05-16

申请号：US10472343

申请日：2002-03-20

申请人： Keith Biggadike ,  Rita Field ,  Stephen Barry Guntrip ,  Brian Edgar Looker

发明人： Keith Biggadike ,  Rita Field ,  Stephen Barry Guntrip ,  Brian Edgar Looker

IPC分类号： C07C311/29 ,  A61K31/18

CPC分类号： C07C311/29

摘要： The present invention relates to novel compounds of formula (I), to a process for their menufacture, to pharmaceutical compositions containing them, and to their use in therapy, in particular their use in the prophylaxis and treatment of respiratory diseases

摘要翻译： 本发明涉及式（I）的新化合物，其制造方法，含有它们的药物组合物及其在治疗中的用途，特别是其在预防和治疗呼吸系统疾病中的用途

公开(公告)号：US6114318A

公开(公告)日：2000-09-05

申请号：US91747

申请日：1998-06-24

申请人： Keith Biggadike ,  Panayiotis Alexandrou Procopiou

发明人： Keith Biggadike ,  Panayiotis Alexandrou Procopiou

IPC分类号： A61K31/505 ,  A61K31/00 ,  A61K31/565 ,  A61P5/30 ,  A61P29/00 ,  C07J71/00

CPC分类号： C07J71/0031

摘要： Compounds of the androstane series are described having the formula (I) and solvates thereof in which R.sub.1 and R.sub.2 are the same or different and each represents hydrogen or C.sub.1-6 alkyl; R.sub.3 and R.sub.4 are the same or different and each represents hydrogen or halogen; and ##STR1## represents a single or a double bond. Compounds of formula (I) and their solvates are useful as anti-inflammatory or anti-allergic agents.

摘要翻译： PCT No.PCT / GB96 / 03138 Sec。 371日期：1998年6月24日 102（e）1998年6月24日PCT 1996年12月19日PCT PCT。 公开号WO97 / 24368 日本1997年7月10日描述了具有式（I）及其溶剂化物的式（I）化合物，其中R 1和R 2相同或不同，各自表示氢或C 1-6烷基; R3和R4相同或不同，各自表示氢或卤素; 并且表示单键或双键。 式（I）化合物及其溶剂化物可用作抗炎或抗过敏剂。

公开(公告)号：US06197761B1

公开(公告)日：2001-03-06

申请号：US09091748

申请日：1998-06-24

申请人： Keith Biggadike ,  Panayiotis Alexandrou Procopiou

发明人： Keith Biggadike ,  Panayiotis Alexandrou Procopiou

IPC分类号： A61K3158

CPC分类号： C07J41/0066 ,  C07J3/005 ,  C07J17/00 ,  C07J31/006

摘要： Compounds of the androstane series are described having general formula and solvates thereof, in which R1 represents O, S or NH; R2 individually represents OC(═O)C1-6 alkyl; R3 individually represents hydrogen, methyl (which may be in either the &agr; or &bgr; configuration) or methylene; or R2 and R3 together represent where R6 and R7 are the same or different and each represents hydrogen or C1-6 alkyl; R4 and R5 are the same or different and each represents hydrogen or halogen and represents a single or a double bond. These compounds and their solvates have use in medicine as anti-inflammatory or anti-allergic agents.

摘要翻译： 具有通式和溶剂合物的雄甾烷系列化合物被描述，其中R 1表示O，S或NH; R2各自表示OC（= O）C 1-6烷基; R3各自表示氢，甲基（其可以是α或β构型）或亚甲基; 或R 2和R 3一起表示其中R 6和R 7相同或不同，并且各自表示氢或C 1-6烷基; R4和R5相同或不同，各自表示氢或卤素，并且表示单键或双键。 这些化合物及其溶剂化物在药物中用作抗炎或抗过敏剂。

公开(公告)号：US08765772B2

公开(公告)日：2014-07-01

申请号：US13058470

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 ,  C07D473/34

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： The present invention relates to 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： 本发明涉及式（I）的化合物：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。