公开(公告)号：WO2006037480A8

公开(公告)日：2006-05-18

申请号：PCT/EP2005010237

申请日：2005-09-22

Applicant: HOFFMANN LA ROCHE ,  DEHMLOW HENRIETTA ,  KUHN BERND ,  PANDAY NARENDRA ,  RATNI HASANE ,  WRIGHT MATTHEW BLAKE

Inventor： DEHMLOW HENRIETTA ,  KUHN BERND ,  PANDAY NARENDRA ,  RATNI HASANE ,  WRIGHT MATTHEW BLAKE

IPC: C07C69/92 ,  A61K31/085 ,  A61K31/192 ,  A61K31/216 ,  A61K31/235 ,  A61K31/421 ,  A61K31/423 ,  A61K31/428 ,  C07C43/23 ,  C07C59/68 ,  C07C65/24 ,  C07C69/734 ,  C07D261/20 ,  C07D263/32 ,  C07D275/04

CPC classification number: C07D275/04 ,  C07C43/23 ,  C07C59/68 ,  C07C65/24 ,  C07C69/734 ,  C07C69/92 ,  C07D249/06 ,  C07D261/08 ,  C07D261/20 ,  C07D263/32

Abstract: The invention is concerned with hexafluoroisopropanol substituted ether derivatives of formula (I), wherein R l to R 3 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds bind to LXR alpha and LXR beta and can be used as medicaments.

Abstract translation: 本发明涉及式（I）的六氟异丙醇取代的醚衍生物，其中R 1至R 3如在说明书和权利要求书中所定义，以及生理学上 可接受的盐和酯。 这些化合物与LXRα和LXRβ结合，可用作药物。

公开(公告)号：WO2006066778A3

公开(公告)日：2006-08-10

申请号：PCT/EP2005013460

申请日：2005-12-14

Applicant: HOFFMANN LA ROCHE ,  BOEHRINGER MARKUS ,  GROEBKE ZBINDEN KATRIN ,  HAAP WOLFGANG ,  HILPERT HANS ,  PANDAY NARENDRA ,  RICKLIN FABIENNE

Inventor： BOEHRINGER MARKUS ,  GROEBKE ZBINDEN KATRIN ,  HAAP WOLFGANG ,  HILPERT HANS ,  PANDAY NARENDRA ,  RICKLIN FABIENNE

IPC: C07D277/46 ,  C07D401/10 ,  C07D409/06 ,  C07D409/14 ,  C07D417/06 ,  C07D417/10 ,  C07D417/14

CPC classification number: C07D401/10 ,  C07D277/46 ,  C07D409/06 ,  C07D409/14 ,  C07D417/06 ,  C07D417/10 ,  C07D417/14

Abstract: The invention is concerned with novel heteroarylacetamides of formula (I) R d -C(O)-N(R e )-R c -CH 2 -C(O)-N(R a )(R b ), wherein R a to R e are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit the coagulation factor Xa and can be used as medicaments.

Abstract translation: 本发明涉及式（I）的新型杂芳基乙酰胺R 2 -C（O）-N（R e） - R c - CH 2 -C（O）-N（R a）a（R b）b）其中R a a至 R e如在说明书和权利要求书中所定义的，以及其生理上可接受的盐。 这些化合物抑制凝血因子Xa，并且可以用作药物。

公开(公告)号：WO2006048152A2

公开(公告)日：2006-05-11

申请号：PCT/EP2005011430

申请日：2005-10-25

Applicant: HOFFMANN LA ROCHE ,  BOEHRINGER MARKUS ,  GROEBKE ZBINDEN KATRIN ,  HAAP WOLFGANG ,  HILPERT HANS ,  HIMBER JACQUES ,  HUMM ROLAND ,  IDING HANS ,  KNOPP DIETMAR ,  PANDAY NARENDRA ,  RICKLIN FABIENNE ,  STAHL CHRISTOPH MARTIN

Inventor： BOEHRINGER MARKUS ,  GROEBKE ZBINDEN KATRIN ,  HAAP WOLFGANG ,  HILPERT HANS ,  HIMBER JACQUES ,  HUMM ROLAND ,  IDING HANS ,  KNOPP DIETMAR ,  PANDAY NARENDRA ,  RICKLIN FABIENNE ,  STAHL CHRISTOPH MARTIN

CPC classification number: C07D213/64 ,  C07D213/75 ,  C07D233/64 ,  C07D279/02 ,  C07D295/135 ,  C07D295/185 ,  C07D401/12

Abstract: The invention is concerned with novel dicarboxamide derivatives of formula (I) wherein A, B, R C , D and E are as defined in the description and in the claims, as well 5as physiologically acceptable salts thereof. These compounds inhibit the coagulation factor Xa and can be used as medicaments.

Abstract translation: 本发明涉及式（I）的新型二甲酰胺衍生物，其中A，B，R，D和E如说明书和权利要求书中所定义，以及其生理上可接受的盐。 这些化合物抑制凝血因子Xa，并且可以用作药物。

公开(公告)号：WO2007054453A3

公开(公告)日：2007-07-19

申请号：PCT/EP2006068012

申请日：2006-11-01

Applicant: HOFFMANN LA ROCHE ,  BOEHRINGER MARKUS ,  GROEBKE ZBINDEN KATRIN ,  HAAP WOLFGANG ,  PANDAY NARENDRA ,  RICKLIN FABIENNE ,  STAHL MARTIN ,  SCHMITZ PETRA

Inventor： BOEHRINGER MARKUS ,  GROEBKE ZBINDEN KATRIN ,  HAAP WOLFGANG ,  PANDAY NARENDRA ,  RICKLIN FABIENNE ,  STAHL MARTIN ,  SCHMITZ PETRA

IPC: C07D401/12 ,  A61K31/40 ,  A61K31/47 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14

CPC classification number: C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14

Abstract: The invention is concerned with novel carbocyclyl fused cyclic amines of formula (I) wherein A, X 1 to X 3 , Y 1 to Y 3 , Z, R 1 , R 2 , m and n are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit the coagulation factor Xa and can be used as medicaments.

Abstract translation: 本发明涉及式（I）的新型碳环稠合环胺，其中A，X 1至X 3，Y 1至Y 1， Z，R 1，R 2，m和n如说明书和权利要求书中所定义，以及生理上可接受的盐 它们。 这些化合物抑制凝血因子Xa，并且可以用作药物。

公开(公告)号：WO2005092856A8

公开(公告)日：2006-12-21

申请号：PCT/EP2005002869

申请日：2005-03-17

Applicant: HOFFMANN LA ROCHE ,  DEHMLOW HENRIETTA ,  KUHN BERND ,  MASCIADRI RAFFAELLO ,  PANDAY NARENDRA ,  RATNI HASANE ,  WRIGHT MATTHEW BLAKE

Inventor： DEHMLOW HENRIETTA ,  KUHN BERND ,  MASCIADRI RAFFAELLO ,  PANDAY NARENDRA ,  RATNI HASANE ,  WRIGHT MATTHEW BLAKE

IPC: A61K31/40 ,  C07D209/70 ,  C07D209/86 ,  C07D209/88 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12 ,  C07D411/06 ,  C07D411/14 ,  C07D413/06 ,  C07D413/14 ,  C07D417/06 ,  C07D471/04

CPC classification number: C07D413/06 ,  C07D209/70 ,  C07D209/88 ,  C07D403/12 ,  C07D413/14 ,  C07D417/06

Abstract: The present invention relates to compounds of the formula (I) wherein R 1 , R 2 , R 3 , R 4 , R 5 , X 1 , X 2 , X 3 , X 4 , n, and k are defined in the description and claims, and pharmaceutically acceptable salts and/or pharmaceutically acceptable esters thereof. The compounds are useful for in the treatment and prophylaxis of diseases which are modulated by LXRa and/or LXRß agonists, including increased lipid and cholesterol levels, particularly low HDL-cholesterol, high LDL-cholesterol, atherosclerotic diseases, diabetes, particularly non-insulin dependent diabetes mellitus, metabolic syndrome, dyslipidemia, Alzheimer's disease, sepsis, inflammatory diseases such as colitis, pancreatitis, cholestasis/fibrosis of the liver, and diseases that have an inflammatory component such as Alzheimer's disease or impaired/improvable cognitive function.

Abstract translation: 本发明涉及式（I）的化合物，其中R 1，R 2，R 3，R 4， 其中，R 5，X 5，X 1，X 2，X 3，X 4， SUP，n和k在说明书和权利要求书中被定义，以及其药学上可接受的盐和/或其药学上可接受的酯。 该化合物可用于治疗和预防由LXRα和/或LXRβ激动剂调节的疾病，包括增加脂质和胆固醇水平，特别是低HDL-胆固醇，高LDL-胆固醇，动脉粥样硬化疾病，糖尿病，特别是非胰​​岛素 依赖性糖尿病，代谢综合征，血脂异常，阿尔茨海默氏病，败血症，炎性疾病如结肠炎，胰腺炎，胆汁淤积/肝纤维化，以及具有炎性成分如阿尔茨海默病和受损/可改善的认知功能的疾病。

公开(公告)号：WO2006114401A2

公开(公告)日：2006-11-02

申请号：PCT/EP2006061776

申请日：2006-04-24

Applicant: HOFFMANN LA ROCHE ,  GROEBKE-ZBINDEN KATRIN ,  HAAP WOLFGANG ,  HILPERT HANS ,  PANDAY NARENDRA ,  RICKLIN FABIENNE ,  WIRZ BEAT

Inventor： GROEBKE-ZBINDEN KATRIN ,  HAAP WOLFGANG ,  HILPERT HANS ,  PANDAY NARENDRA ,  RICKLIN FABIENNE ,  WIRZ BEAT

CPC classification number: C07D207/12 ,  C07D207/14 ,  C07D207/16 ,  C07D401/14 ,  C07D409/14 ,  C07D413/14 ,  C07D513/04

Abstract: The invention is concerned with novel cyclic amines of formula (I) wherein X 1 to X 3 , Y 1 to Y 3 , R 1' , R 1'' and n are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit the coagulation factor Xa and can be used as medicaments.

Abstract translation: 本发明涉及新的式（I）的环胺，其中X 1至X 3，Y 1至Y 3， R 1，R 1，R 1和R 2如在说明书和权利要求书中所定义，以及其生理上可接受的盐。 这些化合物抑制凝血因子Xa，并且可以用作药物。

公开(公告)号：BRPI0718064A2

公开(公告)日：2013-11-05

申请号：BRPI0718064

申请日：2007-10-15

Applicant: HOFFMANN LA ROCHE

Inventor： ZBINDEN KATRIN GROEBKE ,  HAAP WOLFGANG ,  HILPERT HANS ,  KUHN BERND ,  PANDAY NARENDRA ,  RICKLIN FABIENNE

IPC: C07D413/14 ,  A61K31/497 ,  A61P7/02

Abstract: The invention is concerned with novel heteroaryl carboxamides of formula (I) wherein A, R1, R2, X, Y, Z and m are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit the coagulation factor Xa and can be used for the treatment or prevention of thrombotic disorders.

公开(公告)号：AU2006286535B2

公开(公告)日：2012-09-06

申请号：AU2006286535

申请日：2006-08-28

Applicant: HOFFMANN LA ROCHE

Inventor： GROEBKE ZBINDEN KATRIN ,  HILPERT HANS ,  RICKLIN FABIENNE ,  HAAP WOLFGANG ,  PANDAY NARENDRA

IPC: C07D409/12 ,  A61K31/4427 ,  A61K31/5377 ,  A61P7/02 ,  C07D413/12

Abstract: The invention is concerned with novel cycloalkane carboxamides of Formula (I) wherein X, X, Y, Y, R, R, R, R, m and n are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit the coagulation factor Xa and can be used as medicaments.

公开(公告)号：BRPI0618523A2

公开(公告)日：2011-09-06

申请号：BRPI0618523

申请日：2006-11-01

Applicant: HOFFMANN LA ROCHE

Inventor： BOEHRINGER MARKUS ,  ZBINDEN KATRIN GROEBKE ,  HAAP WOLFGANG ,  PANDAY NARENDRA ,  RICKLIN FABIENNE ,  SCHMITZ PETRA ,  STAHL MARTIN

IPC: C07D401/12 ,  A61K31/40 ,  A61K31/47 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14

Abstract: The invention is concerned with novel carbocyclyl fused cyclic amines of formula (I) wherein A, X1 to X3, Y1 to Y3, Z, R1, R2, m and n are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit the coagulation factor Xa and can be used as medicaments.

公开(公告)号：CA2564563C

公开(公告)日：2011-07-05

申请号：CA2564563

申请日：2005-04-26

Applicant: HOFFMANN LA ROCHE

Inventor： DEHMLOW HENRIETTA ,  KUHN BERND ,  PANDAY NARENDRA ,  RATNI HASANE ,  SCHULZ-GASCH TANJA ,  WRIGHT MATTHEW BLAKE

IPC: C07D413/06 ,  A61K31/404 ,  A61P3/06 ,  C07D209/08 ,  C07D209/12 ,  C07D209/30 ,  C07D401/06 ,  C07D403/06 ,  C07D409/06 ,  C07D413/10 ,  C07D417/06

Abstract: Compounds of formula (I) (see formula I) or pharmaceutically acceptable salts or pharmaceutically acceptable esters thereof, wherein R1, R2, R3, R4, R5, R6, A, m, n and p are defined as in claim 1. These compounds can be used as medicaments in the treatment of diseases such as atherosclerosis and diabetes.