公开(公告)号：US20060089375A1

公开(公告)日：2006-04-27

申请号：US10527866

申请日：2003-09-12

Applicant: David Allen ,  Diane Coe ,  Caroline Cook ,  Michael Dowle ,  Christophen Edlin ,  Julie Hamblin ,  Martin Johnson ,  Paul Jones ,  Richard Knowles ,  Mika Lindvall ,  Charlotte Mitchell ,  Alison Redgrave ,  Peter Ward

Inventor： David Allen ,  Diane Coe ,  Caroline Cook ,  Michael Dowle ,  Christophen Edlin ,  Julie Hamblin ,  Martin Johnson ,  Paul Jones ,  Richard Knowles ,  Mika Lindvall ,  Charlotte Mitchell ,  Alison Redgrave ,  Peter Ward

IPC: C07D471/02 ,  A61K31/4745

CPC classification number: C07D471/04

Abstract: The invention relates to a compound of formula (I) or a salt thereof: wherein: R1 is C1-4alkyl, C1-3fluoroalkyl, —CH2CH2OH or —CH2CH2CO2C1-2alkyl; R2 is a hydrogen atom (H), methyl or C1fluoroalkyl; R3 is optionally substituted C3-8cycloalkyl or optionally substituted mono-unsaturated-C5-7cycloalkenyl or an optionally substituted heterocyclic group of sub-formula (aa), (bb) or (cc); in which n1 and n2 independently are 1 or 2; and in which Y is O, S, SO2, or NR10; or R3 is a bicyclic group (dd) or (ee): and wherein X is NR4R5 or OR5a. The compounds are phosphodiesterase (PDE) inhibitors, in particular PDE4 inhibitors. Also provided is the use of a compound of formula (I), or a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for the treatment and/or prophylaxis of an inflammatory and/or allergic disease in a mammal such as a human, for example chronic obstructive pulmonary disease (COPD), asthma, or allergic rhinitis.

Abstract translation: 本发明涉及式（I）化合物或其盐：其中：R 1是C 1-4烷基，C 1-3烷基， 氟代烷基，-CH 2 CH 2 OH或-CH 2 CH 2 CO 2， C 1-12烷基; R 2是氢原子（H），甲基或C 1氟代烷基; R 3是任选取代的C 3-8环烷基或任选取代的单不饱和C 5〜5-7环烯基或任选取代的杂环基 子公式（aa），（bb）或（cc）; 其中n 1和n 2独立地为1或2; 并且其中Y是O，S，SO 2或NR 10; 或R 3是双环基（dd）或（ee）：其中X是NR 4 R 5或OR 5a 。 这些化合物是磷酸二酯酶（PDE）抑制剂，特别是PDE4抑制剂。 还提供了式（I）化合物或其药学上可接受的盐在制备用于治疗和/或预防哺乳动物例如人的炎性和/或过敏性疾病的药物中的用途， 例如慢性阻塞性肺疾病（COPD），哮喘或过敏性鼻炎。

公开(公告)号：US20060063765A1

公开(公告)日：2006-03-23

申请号：US10509162

申请日：2003-03-27

Applicant: Rachael Ancliff ,  Caroline Cook ,  Colin Eldred ,  Paul Gore ,  Lee Harrison ,  Martin Hayes ,  Simon Hodgson ,  Duncan Judd ,  Suzanne Keeling ,  Xiao Lewell ,  Gail Mills ,  Graeme Robertson ,  Stephen Swanson ,  Andrew Walker ,  Mark Wilkinson

Inventor： Rachael Ancliff ,  Caroline Cook ,  Colin Eldred ,  Paul Gore ,  Lee Harrison ,  Martin Hayes ,  Simon Hodgson ,  Duncan Judd ,  Suzanne Keeling ,  Xiao Lewell ,  Gail Mills ,  Graeme Robertson ,  Stephen Swanson ,  Andrew Walker ,  Mark Wilkinson

IPC: A61K31/537 ,  C07D265/30

CPC classification number: C07D413/12 ,  C07D413/14 ,  C07D417/12

Abstract: Compounds of formula (I): wherein: R1 represents substituted or unsubstituted heteroaryl; Y represents —(CRnaRnb)n—; Rna and Rnb are each independently hydrogen or C1-6alkyl; n is an integer from 0 to 5; R2 represents unsubstituted or substituted aryl or unsubstituted or substituted heteroaryl; R3 and R4 each independently represent hydrogen or C1-6alkyl; R7 represents hydrogen or C1-6alkyl; R8 represents hydrogen or C1-6alkyl; and salts and solvates thereof; are CCR3 antagonists and are thus indicated to be useful in therapy.

Abstract translation: 式（I）的化合物：

公开(公告)号：US20060079525A1

公开(公告)日：2006-04-13

申请号：US11284544

申请日：2005-11-22

Applicant: Rachael Ancliff ,  Caroline Cook ,  Colin Eldred ,  Paul Gore ,  Lee Harrison ,  Simon Hodgson ,  Duncan Judd ,  Suzanne Keeling ,  Xiao Lewell ,  Graeme Robertson ,  Stephen Swanson

Inventor： Rachael Ancliff ,  Caroline Cook ,  Colin Eldred ,  Paul Gore ,  Lee Harrison ,  Simon Hodgson ,  Duncan Judd ,  Suzanne Keeling ,  Xiao Lewell ,  Graeme Robertson ,  Stephen Swanson

IPC: A61K31/537 ,  C07D265/30

CPC classification number: C07D265/30 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14

Abstract: There are provided according to the invention, novel compounds of formula (I) wherein R1, R2, R3, R4, R5, X, a, b and Z are as defined in the specification, processes for preparing them, formulations containing them and their use in therapy for the treatment of inflammatory diseases.

Abstract translation: 根据本发明，提供了式（I）的新化合物，其中R 1，R 2，R 3，R 3， 4，R 5，X，a，b和Z如说明书中所定义，制备方法，含有它们的制剂及其在治疗炎性疾病中的用途。

公开(公告)号：US20060058299A1

公开(公告)日：2006-03-16

申请号：US10509417

申请日：2003-03-27

Applicant: Rachael Ancliff ,  Caroline Cook ,  Colin Eldred ,  Paul Gore ,  Lee Harrison ,  Martin Hayes ,  Simon Hodgson ,  Duncan Judd ,  Suzanne Keeling ,  Xiao Lewell ,  Gail Mills ,  Graeme Robertson ,  Stephen Swanson ,  Andrew Walker ,  Mark Wilkinson

Inventor： Rachael Ancliff ,  Caroline Cook ,  Colin Eldred ,  Paul Gore ,  Lee Harrison ,  Martin Hayes ,  Simon Hodgson ,  Duncan Judd ,  Suzanne Keeling ,  Xiao Lewell ,  Gail Mills ,  Graeme Robertson ,  Stephen Swanson ,  Andrew Walker ,  Mark Wilkinson

IPC: C07D265/30 ,  A61K31/537

CPC classification number: C07D265/30 ,  A61K31/5375

Abstract: Compound of formula (I): and salts and solvates thereof, a process for its preparation, pharmaceutical formulations containing it and its use in therapy.

Abstract translation: 式（I）化合物：

公开(公告)号：US20080021058A1

公开(公告)日：2008-01-24

申请号：US10598940

申请日：2005-03-15

Applicant: David Allen ,  Diane Coe ,  Caroline Cook ,  Michael Dowle ,  Christopher Edlin ,  Julie Hamblin ,  Martin Johnson ,  Paul Jones ,  Mika Lindvall ,  Charlotte Mitchell ,  Alison Redgrave ,  Naimisha Trivedi

Inventor： David Allen ,  Diane Coe ,  Caroline Cook ,  Michael Dowle ,  Christopher Edlin ,  Julie Hamblin ,  Martin Johnson ,  Paul Jones ,  Mika Lindvall ,  Charlotte Mitchell ,  Alison Redgrave ,  Naimisha Trivedi

IPC: A61K31/437 ,  A61P29/00 ,  A61P37/08 ,  C07D221/04

CPC classification number: C07D471/04

Abstract: The invention provides a compound of formula (I) or a salt thereof: wherein W is Ar, —CR4R5Ar or a group (y) or (y1), wherein Ar is (x) or (z): R1 is C1-4alkyl, C1-3fluoroalkyl or —CH2CH2OH. R2 is C2-6alkyl, C3-6cycloalkyl or —(CH2)n4-C3-6cycloalkyl; and R3 is optionally substituted C3-8cycloalkyl, optionally substituted mono-unsaturated-C5-7cycloalkenyl, an optionally substituted heterocyclic group (aa), (bb) or (cc) (in which Y is O, S, SO2, or NR10), or a bicyclic group (ee): These compounds are PDE4 inhibitors.

Abstract translation: 本发明提供式（I）化合物或其盐：其中W为Ar，-CR 4 R 5或Ar或基团（y）或（y1） 其中Ar是（x）或（z）：R 1是C 1-4烷基，C 1-3 - 氟代烷基或-CH 2 CH 2 OH。 R 2是C 2-6 - 烷基，C 3-6环烷基或 - （CH 2 CH 2） _{n + 4-C 3-6环烷基; 且R 3是任选取代的C 3-8环烷基，任选取代的单不饱和C 5〜5-7环烯基，任意取代的杂环基 （aa），（bb）或（cc）（其中Y为O，S，SO 2或NR 10）或双环基团（ee） 这些化合物是PDE4抑制剂。}

公开(公告)号：US20070280971A1

公开(公告)日：2007-12-06

申请号：US10598838

申请日：2005-03-15

Applicant: Siegfried Christensen ,  Caroline Cook ,  Christopher Edlin ,  Martin Johnson ,  Paul Jones ,  Mika Lindvall ,  Amyn Sayani ,  Naimisha Trivedi ,  Lionel Trottet

Inventor： Siegfried Christensen ,  Caroline Cook ,  Christopher Edlin ,  Martin Johnson ,  Paul Jones ,  Mika Lindvall ,  Amyn Sayani ,  Naimisha Trivedi ,  Lionel Trottet

IPC: A61K31/437 ,  A61K9/06 ,  A61K9/107 ,  A61P17/00 ,  A61P29/00 ,  A61P37/00 ,  C07D471/04

CPC classification number: C07D471/04

Abstract: The invention provides 4-{[1-(aminocarbonyl)-4-piperidinyl]amino}-N-[(3,4-dimethylphenyl)methyl]-1-ethyl-1H-pyrazolo[3,4-b]pyridine-5-carboxamide, which is the compound of formula (I): or a salt thereof.

Abstract translation: 本发明提供4 - {[1-（氨基羰基）-4-哌啶基]氨基} -N - [（3,4-二甲基苯基）甲基] -1-乙基-1H-吡唑并[3,4-b]吡啶-5 甲酰胺，其为式（I）的化合物或其盐。

公开(公告)号：US20070167485A1

公开(公告)日：2007-07-19

申请号：US10598944

申请日：2005-03-15

Applicant: Diane Coe ,  Caroline Cook ,  Anthony Cooper ,  Christopher Edlin ,  Julie Hamblin ,  Martin Johnson ,  Paul Jones ,  Mika Lindvall ,  Charlotte Mitchell ,  Alison Redgrave ,  John Robinson

Inventor： Diane Coe ,  Caroline Cook ,  Anthony Cooper ,  Christopher Edlin ,  Julie Hamblin ,  Martin Johnson ,  Paul Jones ,  Mika Lindvall ,  Charlotte Mitchell ,  Alison Redgrave ,  John Robinson

IPC: A61K31/44

CPC classification number: C07D471/04

Abstract: The invention relates to a compound of formula (I) or a salt thereof: wherein: R1 is Et, n-Pr, i-Pr, C2fluoroalkyl, or —CH2CH2OH; R2 is H, Me, Et, n-Pr, i-Pr, C1-2fluoroalkyl, cyclopropyl or (cyclopropyl)methyl-; and NHR3 has the sub-formula (nhr3): wherein R3a is methyl or ethyl; R3b is H, methyl or ethyl; R3c is H, methyl or ethyl, R3d is H, methyl or ethyl, and R3e is H or methyl, provided that: (a) R3b is methyl or ethyl; and/or (b) R3c and R3d are independently methyl or ethyl; and provided that: (c) when R3c is ethyl and/or when R3d is ethyl and/or when R3e is methyl, then: R3a is methyl and/or R3b is hydrogen or methyl. These compounds are PDE4 inhibitors.

Abstract translation: 本发明涉及式（I）化合物或其盐：其中：R 1是Et，n-Pr，i-Pr，C 2氟代烷基，或 -CH 2 CH 2 CH 2 OH; R 2是H，Me，Et，n-Pr，i-Pr，C 1-12氟代烷基，环丙基或（环丙基）甲基; 和NHR 3具有子式（nhr3）：其中R 3a是甲基或乙基; R 3b是H，甲基或乙基; R 3c是H，甲基或乙基，R 3d是H，甲基或乙基，R 3e是H或甲基，条件是： （a）R 3b是甲基或乙基; 和/或（b）R 3c和R 3d独立地是甲基或乙基; 并且条件是：（c）当R 3c为乙基时，和/或当R 3d为乙基时，和/或当R 3e为甲基时， 那么：R 3a是甲基，和/或R 3b是氢或甲基。 这些化合物是PDE4抑制剂。