公开(公告)号：WO2013038189A1

公开(公告)日：2013-03-21

申请号：PCT/GB2012/052265

申请日：2012-09-13

Applicant: PROXIMAGEN LTD. ,  CARLEY, Allison ,  SIMPSON, Iain

Inventor： CARLEY, Allison ,  SIMPSON, Iain

IPC: C07D471/04 ,  A61K31/437 ,  A61P29/00 ,  A61P35/00

CPC classification number: C07D471/04

Abstract: Compounds of formula (I) are inhibitors of Semicarbazide-sensitive amine oxidase R 1 -X-R 2 (I) wherein R 1 , X and R 2 are as defined in the claims.

Abstract translation: 式（I）化合物是氨基脲敏感性胺氧化酶R1-X-R2（Ⅰ）的抑制剂，其中R1，X和R2如权利要求中所定义。

公开(公告)号：WO2009147211A1

公开(公告)日：2009-12-10

申请号：PCT/EP2009/056877

申请日：2009-06-04

Applicant: BIOVITRUM AB (publ) ,  HIGGINBOTTOM, Michael ,  SIMPSON, Iain ,  HORTON, James ,  TYZACK, Charles ,  HORGAN, Anne Viet-Anh (nee Nguyen) ,  CHAPMAN, Emma

Inventor： HIGGINBOTTOM, Michael ,  SIMPSON, Iain ,  HORTON, James ,  TYZACK, Charles ,  HORGAN, Anne Viet-Anh (nee Nguyen) ,  CHAPMAN, Emma

IPC: A61K31/4439 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/5377 ,  C07D213/30 ,  C07D213/40 ,  C07D401/12 ,  C07D413/12 ,  A61P3/00

CPC classification number: C07D213/30 ,  C07D213/40 ,  C07D401/12 ,  C07D413/12

Abstract: The present invention relates to new compounds of formula (I), to pharmaceutical compositions comprising these compounds and to the use of these compounds as leptin receptor modulator mimetics in the preparation of medicaments against conditions associated with weight gain, type 2 diabetes and dyslipidemias.

Abstract translation: 本发明涉及新的式（I）化合物，包含这些化合物的药物组合物以及这些化合物作为瘦素受体调节剂模拟物在制备与增重，2型糖尿病和血脂异常相关的病症的药物中的用途。

公开(公告)号：WO2005020987A1

公开(公告)日：2005-03-10

申请号：PCT/GB2004/003648

申请日：2004-08-27

Applicant: ASTRAZENECA AB ,  ASTRAZENECA UK LIMITED ,  BIRCH, Alan, Martin ,  SIMPSON, Iain ,  STOCKER, Andrew ,  WHITTAMORE, Paul, Robert, Owen

Inventor： BIRCH, Alan, Martin ,  SIMPSON, Iain ,  STOCKER, Andrew ,  WHITTAMORE, Paul, Robert, Owen

IPC: A61K31/407

CPC classification number: C07D471/04 ,  C07D495/04

Abstract: Heterocyclic amides of formula (1) wherein: B is selected from R4 and R 5 together are either -S-C(R 6)=C(R 7)_ or _C(R7)=C(R6)_S_; A is a pyridylene ring; m is 0, 1 or 2; n is 0 or 1; R 2 is for example selected from (I -4C)alkyl, hydroxy(l -4C)alkyl, dihydroxy(2-4C)alkyl and (1 -4C)aIkoxy(1 -4C)alkyl. or a pharmaceutically acceptable salt possess glycogen phosphorylase inhibitory activity and accordingly have value in the treatment of disease states associated with increased glycogen phosphorylase activity. Processes for the manufacture of said heterocyclic amide derivatives, intermediates in said processes and pharmaceutical compositions containing the heterocyclic amide derivatives are described.

Abstract translation: 式（1）的杂环酰胺其中：B选自R4和R5一起是-S-C（R 6）= C（R 7）或-C（R 7）= C（R 6） A是吡啶环; m为0,1或2; n为0或1; R 2例如选自（I-4c）烷基，羟基（1-4C）烷基，二羟基（2-4C）烷基和（1-4C）烷氧基（1-4C）烷基。 或药学上可接受的盐具有糖原磷酸化酶抑制活性，因此在治疗与增加的糖原磷酸化酶活性相关的疾病状态方面具有价值。 描述了制备所述杂环酰胺衍生物的方法，所述方法中的中间体和含有杂环酰胺衍生物的药物组合物。

公开(公告)号：WO2005013975A1

公开(公告)日：2005-02-17

申请号：PCT/GB2004/003364

申请日：2004-08-04

Applicant: ASTRAZENECA AB ,  ASTRAZENECA UK LIMITED ,  BIRCH, Alan, Martin ,  BENNETT, Stuart, Norman, Lile ,  GODFREY, Linda ,  SIMPSON, Iain ,  WHITTAMORE, Paul, Robert, Owen

Inventor： BIRCH, Alan, Martin ,  BENNETT, Stuart, Norman, Lile ,  GODFREY, Linda ,  SIMPSON, Iain ,  WHITTAMORE, Paul, Robert, Owen

IPC: A61K31/404

CPC classification number: C07D209/42

Abstract: A compound of the formula (1) or a pharmaceutically-acceptable salt wherein, for example, A is phenylene or heteroarylene; Y is selected from -C(O)R 2 , -C(O)OR 2 , -C(O)NR 2 R 3 , -(1-4C)alkyl [optionally substituted] -(2-4C)alkenyl, -SO 2 NR 2 R 3 , and -S(O) C R 2 (wherein c is 0, 1 or 2); compounds which possess glycogen phosphorylase inhibitory activity and accordingly have value in the treatment of disease states associated with increased glycogen phosphorylase activity. Processes for the manufacture of compounds and pharmaceutical compositions containing them are described.

Abstract translation: 式（1）的化合物或其药学上可接受的盐，其中例如A是亚苯基或亚杂芳基; Y选自-C（O）R 2，-C（O）OR 2，-C（O）NR 2 R 3， - （1-4C）烷基[任意取代的] （2-4C）烯基，-SO 2 NR 2 R 3和-S（O）CR 2（其中c为0,1或2）; 具有糖原磷酸化酶抑制活性的化合物，因此具有与增加的糖原磷酸化酶活性相关的疾病状态的治疗价值。 描述了制备含有它们的化合物和药物组合物的方法。

公开(公告)号：WO02074287A3

公开(公告)日：2003-05-01

申请号：PCT/GB0201162

申请日：2002-03-14

Applicant: AMURA LTD ,  SIMPSON IAIN ,  PFAENDLER HANS RUDOLF

Inventor： SIMPSON IAIN ,  PFAENDLER HANS RUDOLF

IPC: A61K31/43 ,  A61K45/06 ,  A61P31/04 ,  A61K31/546 ,  A61K31/423 ,  A61K38/14

CPC classification number: A61K45/06 ,  A61K31/43 ,  A61K2300/00

Abstract: Disclosed is use of an oxenpenem-3-carboxylic acid of structure (I) or (II) as define above, in combination with an antibiotic and a pharmaceutically acceptable excipient, to prepare a medicament to treat an infection in a human or animal subject caused by a bacterium which does not produce a significant amount of beta -lactamase.

Abstract translation: 公开了如上定义的结构（I）或（II）的亚苄孕烯-3-羧酸与抗生素和药学上可接受的赋形剂的组合，以制备治疗人或动物受试者感染的药物 通过不产生显着量的β-内酰胺酶的细菌。

公开(公告)号：WO2012049277A1

公开(公告)日：2012-04-19

申请号：PCT/EP2011/067946

申请日：2011-10-13

Applicant: PROXIMAGEN LTD ,  BROWN, Giles ,  HIGGINBOTTOM, Michael ,  STEWART, Alison ,  PATIENT, Lee ,  CARLEY, Allison ,  SIMPSON, Iain ,  SAVORY, Edward Daniel ,  OLIVER, Kathryn ,  COLE, Andrew, Graham

Inventor： BROWN, Giles ,  HIGGINBOTTOM, Michael ,  STEWART, Alison ,  PATIENT, Lee ,  CARLEY, Allison ,  SIMPSON, Iain ,  SAVORY, Edward Daniel ,  OLIVER, Kathryn ,  COLE, Andrew, Graham

IPC: C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  A61K31/551 ,  A61P29/00

CPC classification number: C07D471/08 ,  A61K45/06 ,  C07B59/002 ,  C07B2200/05 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04

Abstract: The compounds of formula (I) are antagonists of the CXCR4 receptor Wherein R 1 , X, Y and R 2 are as defined in the claims.

Abstract translation: 式（I）化合物是CXCR4受体的拮抗剂，其中R1，X，Y和R2如权利要求中所定义。

公开(公告)号：WO2010049731A1

公开(公告)日：2010-05-06

申请号：PCT/GB2009/051447

申请日：2009-10-28

Applicant: ASTRAZENECA AB ,  ASTRAZENECA UK LIMITED ,  DUCRAY, Richard ,  JONES, Clifford, David ,  JUNG, Frédéric, Henri ,  SIMPSON, Iain

Inventor： DUCRAY, Richard ,  JONES, Clifford, David ,  JUNG, Frédéric, Henri ,  SIMPSON, Iain

IPC: C07D471/04 ,  A61K31/437 ,  A61P35/00

CPC classification number: C07D471/04

Abstract: There is provided novel pyrimidine derivatives of formula (I) or pharmaceutically acceptable salts thereof, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.

Abstract translation: 提供式（I）的新型嘧啶衍生物或其药学上可接受的盐，其制备方法，含有它们的药物组合物及其在治疗中的用途。

公开(公告)号：WO2009147219A1

公开(公告)日：2009-12-10

申请号：PCT/EP2009/056892

申请日：2009-06-04

Applicant: BIOVITRUM AB (publ) ,  SIMPSON, Iain ,  HIGGINBOTTOM, Michael ,  HORGAN, Anne Viet-Anh (nee Nguyen) ,  CHAPMAN, Emma

Inventor： SIMPSON, Iain ,  HIGGINBOTTOM, Michael ,  HORGAN, Anne Viet-Anh (nee Nguyen) ,  CHAPMAN, Emma

IPC: C07D211/34 ,  A61K31/445 ,  A61P3/04

CPC classification number: C07D211/34

Abstract: The present invention relates to new compounds of formula (I), to pharmaceutical compositions comprising these compounds and to the use of these compounds as leptin receptor modulator mimetics in the preparation of medicaments against conditions associated with weight gain, type 2 diabetes and dyslipidemias.

Abstract translation: 本发明涉及新的式（I）化合物，包含这些化合物的药物组合物以及这些化合物作为瘦素受体调节剂模拟物在制备与增重，2型糖尿病和血脂异常相关的病症的药物中的用途。

公开(公告)号：WO2008003958A3

公开(公告)日：2008-03-06

申请号：PCT/GB2007002490

申请日：2007-07-05

Applicant: ASTRAZENECA AB ,  ASTRAZENECA UK LTD ,  HALSALL CHRISTOPHER THOMAS ,  RUDGE DAVID ALAN ,  SIMPSON IAIN ,  WARD RICHARD ANDREW

Inventor： HALSALL CHRISTOPHER THOMAS ,  RUDGE DAVID ALAN ,  SIMPSON IAIN ,  WARD RICHARD ANDREW

IPC: C07D487/04 ,  A61K31/522

CPC classification number: C07D487/04 ,  C07D519/00

Abstract: There is provided a compound of formula (I):processes for the manufacure thereof, pharmaceutical compoitions thereof and uses in therapy.

Abstract translation: 提供了式（I）化合物：其制备方法，药物组合物和治疗用途。

公开(公告)号：WO2007135374A1

公开(公告)日：2007-11-29

申请号：PCT/GB2007/001806

申请日：2007-05-16

Applicant: ASTRAZENECA AB ,  ASTRAZENECA UK LIMITED ,  SIMPSON, Iain ,  WARD, Richard, Andrew

Inventor： SIMPSON, Iain ,  WARD, Richard, Andrew

IPC: C07D475/00

CPC classification number: C07D475/00

Abstract: Compounds of formula (I), or optionally the pharmacologically acceptable acid addition salts thereof, and their use in the inhibition of PLK activity are described.

Abstract translation: 描述了式（I）化合物或任选其药理学上可接受的酸加成盐，以及它们在抑制PLK活性中的用途。