公开(公告)号：US07745462B2

公开(公告)日：2010-06-29

申请号：US10552023

申请日：2004-04-02

Applicant: Robin Alec Fairhurst ,  David Andrew Sandham ,  David Beattie ,  Ian Bruce ,  Bernard Cuenoud ,  Reamonn Madden ,  Neil John Press ,  Roger John Taylor ,  Katharine Louise Turner ,  Simon James Watson

Inventor： Robin Alec Fairhurst ,  David Andrew Sandham ,  David Beattie ,  Ian Bruce ,  Bernard Cuenoud ,  Reamonn Madden ,  Neil John Press ,  Roger John Taylor ,  Katharine Louise Turner ,  Simon James Watson

IPC: A61K31/02 ,  C07D215/38

CPC classification number: C07D215/227 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  C07D417/14

Abstract: Compounds of formula I in free or salt form, wherein —C—Y—, R1 and R2 are G have the meanings as indicated in the specification, are useful for treating conditions that are prevented or alleviated by activation of the β2-adrenoreceptor. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.

Abstract translation: 游离或盐形式的式I化合物，其中-C-Y-，R 1和R 2为G具有本说明书中指出的含义，可用于治疗通过活化2-肾上腺素受体而预防或缓解的病症 。 还描述了含有化合物的药物组合物和制备该化合物的方法。

公开(公告)号：US20090209552A1

公开(公告)日：2009-08-20

申请号：US12304576

申请日：2007-06-11

Applicant: David Andrew Sandham ,  Catherine Leblanc ,  Claire Adcock ,  Kamlesh Jagdis Bala ,  Maude Nadine Pierrette Pipet

Inventor： David Andrew Sandham ,  Catherine Leblanc ,  Claire Adcock ,  Kamlesh Jagdis Bala ,  Maude Nadine Pierrette Pipet

IPC: A61K31/496 ,  C07D401/14

CPC classification number: C07D401/12

Abstract: There are provided according to the invention compounds of formula (I) in free or salt form, wherein R3, R4, R5, R6a, R6b, Q and W are as described in the specification, process for preparing them, and their use as pharmaceuticals.

Abstract translation: 根据本发明，提供游离或盐形式的式（I）化合物，其中R3，R4，R5，R6a，R6b，Q和W如说明书中所述，其制备方法及其作为药物的用途 。

公开(公告)号：US20080312229A1

公开(公告)日：2008-12-18

申请号：US12096453

申请日：2006-12-07

Applicant: David Andrew Sandham ,  Catherine Leblanc ,  Harinder Pal Singh ,  Lyndon Nigel Brown

Inventor： David Andrew Sandham ,  Catherine Leblanc ,  Harinder Pal Singh ,  Lyndon Nigel Brown

IPC: A61K31/437 ,  A61P25/00 ,  A61P29/00 ,  A61P37/00 ,  A61P19/00 ,  C07D471/04 ,  A61K31/5377

CPC classification number: C07D471/04

Abstract: There are provided according to the invention compounds of formula (I) in free or salt form, wherein R1, R2, R4, R5, R6, A, D, X, W, m and n are as described in the specification, process for preparing them, and their use as pharmaceuticals.

Abstract translation: 根据本发明，提供游离或盐形式的式（I）化合物，其中R 1，R 2，R 4，R 5，R 6，A，D，X，W，m和n如说明书中所述， 准备他们，并用作药物。

公开(公告)号：US20080269335A1

公开(公告)日：2008-10-30

申请号：US11568464

申请日：2005-05-03

Applicant: David Andrew Sandham ,  Katharine Louise Turner ,  Catherine Leblanc

Inventor： David Andrew Sandham ,  Katharine Louise Turner ,  Catherine Leblanc

IPC: A61K31/19 ,  C07C57/30 ,  A61P11/06 ,  A61P29/00 ,  A61P37/08 ,  A61P37/06

CPC classification number: C07C51/09 ,  C07C59/72 ,  C07C67/11 ,  C07C69/712 ,  C07C255/54 ,  C07C2601/14

Abstract: There are provided according to the invention compounds of formula (I) in free or salt form, wherein R , R , R , X, Y, Z, m, and n are as described in the specification, process for preparing them, and their use as pharmaceuticals.

Abstract translation: 根据本发明，提供游离或盐形式的式（I）化合物，其中R 1，R 2，R 3，X，Y，Z，m和n如 规格，制备方法及其作为药物的用途。

公开(公告)号：US07019136B2

公开(公告)日：2006-03-28

申请号：US10937639

申请日：2004-09-09

Applicant: Gurdip Bhalay ,  Stephen Paul Collingwood ,  Robin Alec Fairhurst ,  Sylvie Felicite Gomez ,  Reto Naef ,  David Andrew Sandham

Inventor： Gurdip Bhalay ,  Stephen Paul Collingwood ,  Robin Alec Fairhurst ,  Sylvie Felicite Gomez ,  Reto Naef ,  David Andrew Sandham

IPC: C07D239/02

CPC classification number: C07D239/545 ,  A61K31/522 ,  C07D473/04 ,  C07D473/06

Abstract: A compound of formula (I): R1 is hydrogen or alkyl optionally substituted by hydroxy, alkoxy, or alkylthio, R2 is hydrogen, alkyl, hydroxyalkyl, alkylcarbonyloxyalkyl, alkoxyalkyl, alkylthioalkyl, alkenyl, cycloalkylalkyl, heterocyclylalkyl, aralkyl in which the aryl ring thereof is optionally fused to a 5-membered heterocyclic group or is optionally substituted by one or more substituents selected from alkoxy, amino, alkylamino, dialkylamino, acylamino, halogen, hydroxy, aminosulfonyl, alkylaminosulfonyl, dialkylaminosulfonyl, alkylsulfonylamino or dialkylaminosulfonylamino, R3 is hydrogen or alkyl optionally substituted by hydroxy, alkoxy, or alkylthio, R4 is hydrogen or alkyl, R5 is a quinolinyl, isoquinolinyl or oxodihydroisoquinolinyl group optionally fused to a 5-membered heterocyclic group and optionally substituted by one or more substituents selected from halogen, cyano, hydroxy, alkyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkoxy, alkylthio, alkenyl, alkoxycarbonyl, alkynyl, carboxyl, acyl, a group of formula —N(R6)R7, aryl optionally substituted by one or more substituents selected from halogen or alkoxy, or heteroaryl having 5 or 6 ring atoms attached through a ring carbon atom to the indicated carbon atom, and R6 and R7 are each independently hydrogen or alkyl optionally substituted by hydroxy or alkoxy or one of R6 and R7 is hydrogen and the other is acyl, or R6 and R7 together with the nitrogen atom to which they are attached denote a 5- or 6-membered heterocyclyl group.

Abstract translation: 式（I）化合物：R 1是氢或任选被羟基，烷氧基或烷硫基取代的烷基，R 2是氢，烷基，羟基烷基，烷基羰氧基烷基，烷氧基烷基 ，烷基硫代烷基，烯基，环烷基烷基，杂环基烷基，芳烷基，其中其芳基环任选地与5元杂环基稠合，或任选地被一个或多个选自烷氧基，氨基，烷基氨基，二烷基氨基，酰氨基，卤素，羟基 ，氨基磺酰基，烷基氨基磺酰基，二烷基氨基磺酰基，烷基磺酰基氨基或二烷基氨基磺酰基氨基，R 3是氢或任选被羟基，烷氧基或烷硫基取代的烷基，R 4是氢或烷基， 任选地与5元杂环基稠合的喹啉基，异喹啉基或氧代二氢异喹啉基，任选地被一个或多个选自卤素，氰基，羟基，烷基，羟烷基，烷氧基烷基，烷硫基 烷基，烷氧基，烷硫基，烯基，烷氧基羰基，炔基，羧基，酰基，式-N（R 6）R 7的基团，任选地被一个或多个 选自卤素或烷氧基的取代基或具有5或6个环原子通过环碳原子连接到指定碳原子的杂芳基，R 6和R 7各自独立地 任选被羟基或烷氧基取代的氢或烷基或R 6和R 7中的一个是氢，另一个是酰基或R 6和 R 7与它们所连接的氮原子一起表示5-或6-元杂环基。

公开(公告)号：US20160168119A1

公开(公告)日：2016-06-16

申请号：US14906187

申请日：2014-07-16

Applicant: Urs BAETTIG ,  David BEATTIE ,  Darren Mark LEGRAND ,  Andrew Stuart LISTER ,  Jeffrey MCKENNA ,  David William PEARCE ,  David Andrew SANDHAM ,  Emily STANLEY ,  Oliver Ross STEWARD ,  Christopher THOMSON

Inventor： Urs BAETTIG ,  David BEATTIE ,  Darren Mark LEGRAND ,  Andrew Stuart LISTER ,  Jeffrey MCKENNA ,  David William PEARCE ,  David Andrew SANDHAM ,  Emily STANLEY ,  Oliver Ross STEWARD ,  Christopher THOMSON

IPC: C07D401/12 ,  C07D403/12 ,  C07D257/04 ,  C07D405/12 ,  C07D417/12 ,  C07D413/12

CPC classification number: C07D401/12 ,  A61K45/06 ,  C07D257/04 ,  C07D403/12 ,  C07D405/12 ,  C07D407/12 ,  C07D413/12 ,  C07D417/12

Abstract: The present invention relates to novel compounds that are autotaxin inhibitors, processes for their preparation, pharmaceutical compositions and medicaments containing them and to their use in diseases and disorders mediated by autotaxin.

公开(公告)号：US08455645B2

公开(公告)日：2013-06-04

申请号：US12699723

申请日：2010-02-03

Applicant: Kamlesh Jagdis Bala ,  Catherine Leblanc ,  David Andrew Sandham ,  Katharine Louise Turner ,  Simon James Watson ,  Lyndon Nigel Brown ,  Brian Cox

Inventor： Kamlesh Jagdis Bala ,  Catherine Leblanc ,  David Andrew Sandham ,  Katharine Louise Turner ,  Simon James Watson ,  Lyndon Nigel Brown ,  Brian Cox

IPC: C07D471/02 ,  A61K31/44

CPC classification number: C07D471/04 ,  A61K31/437 ,  A61K45/06

Abstract: There are provided according to the invention compounds of formula (I), in free or salt form, wherein R1, R2, R3, R4, R5, R6, Q, W, X, m, n and p are as described in the specification, process for preparing them, and their use as pharmaceuticals.

Abstract translation: 根据本发明，提供游离或盐形式的式（I）化合物，其中R 1，R 2，R 3，R 4，R 5，R 6，Q，W，X，m，n和p如说明书 制备方法，以及作为药物的用途。

公开(公告)号：US07678826B2

公开(公告)日：2010-03-16

申请号：US11915168

申请日：2006-05-22

Applicant: Jake Axford ,  Urs Baettig ,  Brian Cox ,  Kamlesh Jagdis Bala ,  Catherine LeBlanc ,  David Andrew Sandham

Inventor： Jake Axford ,  Urs Baettig ,  Brian Cox ,  Kamlesh Jagdis Bala ,  Catherine LeBlanc ,  David Andrew Sandham

IPC: A01N43/36

CPC classification number: C07D295/185

Abstract: Compounds of formula (I) in free or pharmaceutically acceptable salt form, where R1, R2, R3, R4, R5, R6, R7, m, n, w, X, and Y have the meanings as indicated in the specification, are useful for treating conditions mediated by the CRTh2 receptor, especially inflammatory or obstructive airways diseases.

Abstract translation: 其中R 1，R 2，R 3，R 4，R 5，R 6，R 7，m，n，w，X和Y具有如说明书中所示的含义的游离或药学上可接受的盐形式的式（I） 用于治疗由CRTh2受体介导的病症，特别是炎性或阻塞性气道疾病。

公开(公告)号：US20080312230A1

公开(公告)日：2008-12-18

申请号：US12097326

申请日：2006-12-11

Applicant: David Andrew Sandham

Inventor： David Andrew Sandham

IPC: A61K31/5377 ,  A61K31/437 ,  C07D471/04 ,  C07D413/14 ,  A61P25/00

CPC classification number: C07D471/04

Abstract: There are provided according to the invention compounds of formula (I), in free or salt form, wherein R1, R2R3R4, R5, R6, Q, X, m, n, and p are as described in the specification, on process for preparing them, and their use in the manufacture of a medicament for the treatment of neuropathic pain.

Abstract translation: 根据本发明，提供游离或盐形式的式（I）化合物，其中R1，R2R3R4，R5，R6，Q，X，m，n和p如说明书中所述，关于制备方法 它们以及它们在制备用于治疗神经性疼痛的药物中的用途。

公开(公告)号：US06921757B2

公开(公告)日：2005-07-26

申请号：US10312021

申请日：2001-06-26

Applicant: Bernard Cuenoud ,  David Beattie ,  Thomas Hugo Keller ,  Gaynor Elizabeth Pilgrim ,  David Andrew Sandham ,  Simon James Watson

Inventor： Bernard Cuenoud ,  David Beattie ,  Thomas Hugo Keller ,  Gaynor Elizabeth Pilgrim ,  David Andrew Sandham ,  Simon James Watson

IPC: A61K31/56 ,  A61P11/08 ,  A61P29/00 ,  A61P43/00 ,  C07C401/00 ,  C07J3/00 ,  C07J17/00 ,  C07J33/00 ,  C07J41/00 ,  C07J43/00 ,  C07J71/00 ,  A61K31/58

CPC classification number: C07J41/0038 ,  C07J3/005 ,  C07J17/00 ,  C07J33/002 ,  C07J41/0094 ,  C07J43/003 ,  C07J71/0015

Abstract: Compounds of formula (I), where R is a monovalent cyclic organic group having from 3 to 15 atoms in the ring system, useful as pharmaceuticals

Abstract translation: 式（I）化合物，其中R是环系中具有3至15个原子的一价环状有机基团，可用作药物