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：WO2012112958A3

公开(公告)日：2012-11-22

申请号：PCT/US2012025745

申请日：2012-02-17

Applicant: BROAD INST INC ,  GEN HOSPITAL CORP ,  BRIGHAM & WOMENS HOSPITAL ,  HARVARD COLLEGE ,  SLOAN KETTERING INST CANCER ,  DANA FARBER CANCER INST INC ,  HARTWELL KIMBERLY ,  GILLILAND D GARY ,  MOORE MALCOME ,  SCADDEN DAVID ,  SCHREIBER STUART ,  GOLUB TODD ,  EBERT BENJAMIN ,  CARPENTER VAN DYK ANNE ,  LOGAN DAVID ,  STERN ANDREW ,  MILLER PETER ,  NEGRI JOSEPH ,  TOLLIDAY NICOLA ,  STEWART ALISON ,  SHAMJI ALYKHAN ,  MUKHERJEE SIDDHARTHA

Inventor： HARTWELL KIMBERLY ,  GILLILAND D GARY ,  MOORE MALCOME ,  SCADDEN DAVID ,  SCHREIBER STUART ,  GOLUB TODD ,  EBERT BENJAMIN ,  CARPENTER VAN DYK ANNE ,  LOGAN DAVID ,  STERN ANDREW ,  MILLER PETER ,  NEGRI JOSEPH ,  TOLLIDAY NICOLA ,  STEWART ALISON ,  SHAMJI ALYKHAN ,  MUKHERJEE SIDDHARTHA

IPC: G01N33/15 ,  C12N5/071 ,  G06T7/00

CPC classification number: G01N33/5011 ,  A61K31/167 ,  A61K31/22 ,  A61K31/366 ,  A61K31/395 ,  A61K31/405 ,  A61K31/4184 ,  A61K31/423 ,  A61K31/428 ,  A61K31/437 ,  A61K31/4418 ,  A61K31/444 ,  A61K31/4745 ,  A61K31/704 ,  A61K45/06

Abstract: This invention relates to high-throughput, semi-automated methods for identifying compounds that are effective in targeting leukemia stem cells, as well as compounds identified by those methods and uses thereof for treating leukemia.

Abstract translation: 本发明涉及用于鉴定有效靶向白血病干细胞的化合物的高通量，半自动化方法，以及通过这些方法鉴定的化合物及其用于治疗白血病的用途。

公开(公告)号：WO2012112958A2

公开(公告)日：2012-08-23

申请号：PCT/US2012/025745

申请日：2012-02-17

Applicant: THE BROAD INSTITUTE, INC ,  THE GENERAL HOSPITAL CORPORATION ,  THE BRIGHAM AND WOMEN'S HOSPITAL, INC. ,  PRESIDENT AND FELLOWS OF HARVARD COLLEGE ,  SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH ,  DANA FARBER CANCER INSTITUTE, INC. ,  HARTWELL, Kimberly ,  GILLILAND, D. Gary ,  MOORE, Malcome ,  SCADDEN, David ,  SCHREIBER, Stuart ,  GOLUB, Todd ,  EBERT, Benjamin ,  CARPENTER VAN DYK, Anne ,  LOGAN, David ,  STERN, Andrew ,  MILLER, Peter ,  NEGRI, Joseph ,  TOLLIDAY, Nicola ,  STEWART, Alison ,  SHAMJI, Alykhan ,  MUKHERJEE, Siddhartha

Inventor： HARTWELL, Kimberly ,  GILLILAND, D. Gary ,  MOORE, Malcome ,  SCADDEN, David ,  SCHREIBER, Stuart ,  GOLUB, Todd ,  EBERT, Benjamin ,  CARPENTER VAN DYK, Anne ,  LOGAN, David ,  STERN, Andrew ,  MILLER, Peter ,  NEGRI, Joseph ,  TOLLIDAY, Nicola ,  STEWART, Alison ,  SHAMJI, Alykhan ,  MUKHERJEE, Siddhartha

IPC: G01N33/15 ,  C12N5/071 ,  G06T7/00

CPC classification number: G01N33/5011 ,  A61K31/167 ,  A61K31/22 ,  A61K31/366 ,  A61K31/395 ,  A61K31/405 ,  A61K31/4184 ,  A61K31/423 ,  A61K31/428 ,  A61K31/437 ,  A61K31/4418 ,  A61K31/444 ,  A61K31/4745 ,  A61K31/704 ,  A61K45/06

Abstract: This invention relates to high-throughput, semi-automated methods for identifying compounds that are effective in targeting leukemia stem cells, as well as compounds identified by those methods and uses thereof for treating leukemia.

Abstract translation: 本发明涉及用于鉴定有效靶向白血病干细胞的化合物的高通量半自动化方法，以及通过这些方法鉴定的化合物及其用于治疗白血病的用途。

公开(公告)号：WO2011113798A2

公开(公告)日：2011-09-22

申请号：PCT/EP2011053818

申请日：2011-03-14

Applicant: PROXIMAGEN LTD ,  EVANS DAVID ,  CARLEY ALLISON ,  STEWART ALISON ,  HIGGINBOTTOM MICHAEL ,  SAVORY EDWARD ,  SIMPSON IAIN ,  NILSSON MARIANNE ,  HARALDSSON MARTIN ,  NORDLING ERIK ,  KOOLMEISTER TOBIAS

Inventor： EVANS DAVID ,  CARLEY ALLISON ,  STEWART ALISON ,  HIGGINBOTTOM MICHAEL ,  SAVORY EDWARD ,  SIMPSON IAIN ,  NILSSON MARIANNE ,  HARALDSSON MARTIN ,  NORDLING ERIK ,  KOOLMEISTER TOBIAS

IPC: C07D471/04

CPC classification number: C07D471/04 ,  C07D487/04 ,  C07D491/08 ,  C07D498/08 ,  C07D519/00

Abstract: Compounds of formula (I) are inhibitors of Semicarbazide-sensitive amine oxidase wherein R1, A, X and R2 are as defined in the claims.

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

公开(公告)号：WO2013037411A1

公开(公告)日：2013-03-21

申请号：PCT/EP2011/065967

申请日：2011-09-14

Applicant: PROXIMAGEN LIMITED ,  EVANS, David ,  CARLEY, Allison ,  STEWART, Alison ,  HIGGINBOTTOM, Michael ,  SAVORY, Edward ,  SIMPSON, Iain ,  NILSSON, Marianne ,  HARALDSSON, Martin ,  NORDLING, Erik ,  KOOLMEISTER, Tobias

Inventor： EVANS, David ,  CARLEY, Allison ,  STEWART, Alison ,  HIGGINBOTTOM, Michael ,  SAVORY, Edward ,  SIMPSON, Iain ,  NILSSON, Marianne ,  HARALDSSON, Martin ,  NORDLING, Erik ,  KOOLMEISTER, Tobias

IPC: C07D471/04 ,  A61K31/437

CPC classification number: C07D471/04

Abstract: 2-{4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}ethan-1-amine; 3- aminopropyl 4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidine-1-carboxylate; 1-{4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}-4- (dimethylamino)butan-1-one; 5-amino-1-{4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3- yl]piperidin-1-yl}pentan-1-one; N-(2-aminoethyl)-4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3- c]pyridin-3-yl]piperidine-1-carboxamide; N-(3-aminopropyl)-4-[1-(4-chlorophenyl)-1H- pyrrolo[2,3-c]pyridin-3-yl]piperidine-1-carboxamide; 4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3- c]pyridin-3-yl]-N-[3-(dimethylamino)propyl]piperidine-1-carboxamide; 1-({4-[1-(4- chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}carbonyl)piperazine; 4-({4-[1-(4- chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}carbonyl)morpholine; 1-({4-[1-(4- chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}carbonyl)-1,4-diazepane; ethyl 1- [1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidine-4-carboxylate; ethyl 1-[1-(4- methylphenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidine-4-carboxylate; 1-[1-(4- chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidine-4-carboxylic acid; N-(2- aminoethyl)-1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidine-4-carboxamide; 4-({1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidin-4 yl}carbonyl)morpholine; 1-({1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidin- 4-yl}carbonyl)piperazine; {4-[1-(4-methylphenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]morpholin- 3-yl}methanol; {4-[1-(4-methylphenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]morpholin-2-yl}methanol; [(3R)-4-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]morpholin-3- yl]methanol; methyl 4-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]morpholine-3- carboxylate; N-(2-aminoethyl)-4-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3- yl]morpholine-3-carboxamide; 2-{4-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3- yl]morpholin-3-yl}ethan-1-ol; methyl 1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3- yl]piperidine-2-carboxylate; N-(2-aminoethyl)-1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4- c]pyridin-3-yl]piperidine-2-carboxamide; 1-({1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4- c]pyridin-3-yl]piperidin-2-yl}carbonyl)piperazine; 4-[1-(4-methylphenyl)-1H-pyrrolo[2,3- c]pyridin-3-yl]morpholine; 1-(4-chlorophenyl)-3-(piperidin-4-yl)-1H-pyrrolo[2,3-c]pyridin-4- ol; N-butyl-1-(4-chlorophenyl)-N-methyl-1H-pyrazolo[3,4-c]pyridin-3-amine; 1-[4- (fluoromethyl)phenyl]-3-(oxan-4-yl)-1H-pyrazolo[3,4-c]pyridine; and 3-({4-[1-(4- chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidin-1-yl}methyl)pyridine are useful for the inhibition of SSAO activity.

Abstract translation: 2- {4- [1-（4-氯苯基）-1H-吡咯并[2,3-c]吡啶-3-基]哌啶-1-基}乙-1-胺; 4- [1-（4-氯苯基）-1H-吡咯并[2,3-c]吡啶-3-基]哌啶-1-甲酸3-氨基丙酯; 1- {4- [1-（4-氯苯基）-1H-吡咯并[2,3-c]吡啶-3-基]哌啶-1-基} -4-（二甲基氨基）丁-1-酮; 5-氨基-1- {4- [1-（4-氯苯基）-1H-吡咯并[2,3-c]吡啶-3-基]哌啶-1-基}戊-1-酮; N-（2-氨基乙基）-4- [1-（4-氯苯基）-1H-吡咯并[2,3-c]吡啶-3-基]哌啶-1-甲酰胺; N-（3-氨基丙基）-4- [1-（4-氯苯基）-1H-吡咯并[2,3-c]吡啶-3-基]哌啶-1-甲酰胺; 4- [1-（4-氯苯基）-1H-吡咯并[2,3-c]吡啶-3-基] -N- [3-（二甲基氨基）丙基]哌啶-1-甲酰胺; 1 - （{4- [1-（4-氯苯基）-1H-吡咯并[2,3-c]吡啶-3-基]哌啶-1-基}羰基）哌嗪; 4 - （{4- [1-（4-氯苯基）-1H-吡咯并[2,3-c]吡啶-3-基]哌啶-1-基}羰基）吗啉; 1 - （{4- [1-（4-氯苯基）-1H-吡咯并[2,3-c]吡啶-3-基]哌啶-1-基}羰基）-1,4-二氮杂环庚烷; 1- [1-（4-氯苯基）-1H-吡唑并[3,4-c]吡啶-3-基]哌啶-4-甲酸乙酯; 1- [1-（4-甲基苯基）-1H-吡唑并[3,4-c]吡啶-3-基]哌啶-4-甲酸乙酯; 1- [1-（4-氯苯基）-1H-吡唑并[3,4-c]吡啶-3-基]哌啶-4-甲酸; N-（2-氨基乙基）-1- [1-（4-氯苯基）-1H-吡唑并[3,4-c]吡啶-3-基]哌啶-4-甲酰胺; 4 - （{1- [1-（4-氯苯基）-1H-吡唑并[3,4-c]吡啶-3-基]哌啶-4-基}羰基）吗啉; 1 - （{1- [1-（4-氯苯基）-1H-吡唑并[3,4-c]吡啶-3-基]哌啶-4-基}羰基）哌嗪; {4- [1-（4-甲基苯基）-1H-吡唑并[3,4-c]吡啶-3-基]吗啉-3-基}甲醇; {4- [1-（4-甲基苯基）-1H-吡唑并[3,4-c]吡啶-3-基]吗啉-2-基}甲醇; [（3R）-4- [1-（4-氯苯基）-1H-吡唑并[3,4-c]吡啶-3-基]吗啉-3-基]甲醇; 4- [1-（4-氯苯基）-1H-吡唑并[3,4-c]吡啶-3-基]吗啉-3-羧酸甲酯; N-（2-氨基乙基）-4- [1-（4-氯苯基）-1H-吡唑并[3,4-c]吡啶-3-基]吗啉-3-甲酰胺; 2- {4- [1-（4-氯苯基）-1H-吡唑并[3,4-c]吡啶-3-基]吗啉-3-基}乙-1-醇; 1- [1-（4-氯苯基）-1H-吡唑并[3,4-c]吡啶-3-基]哌啶-2-甲酸甲酯; N-（2-氨基乙基）-1- [1-（4-氯苯基）-1H-吡唑并[3,4-c]吡啶-3-基]哌啶-2-甲酰胺; 1 - （{1- [1-（4-氯苯基）-1H-吡唑并[3,4-c]吡啶-3-基]哌啶-2-基}羰基）哌嗪; 4- [1-（4-甲基苯基）-1H-吡咯并[2,3-c]吡啶-3-基]吗啉; 1-（4-氯苯基）-3-（哌啶-4-基）-1H-吡咯并[2,3-c]吡啶-4-醇; N-丁基-1-（4-氯苯基）-N-甲基-1H-吡唑并[3,4-c]吡啶-3-胺; 1- [4-（氟甲基）苯基] -3-（氧代-4-基）-1H-吡唑并[3,4-c]吡啶; 和3 - （{4- [1-（4-氯苯基）-1H-吡唑并[3,4-c]吡啶-3-基]哌啶-1-基}甲基）吡啶可用于抑制SSAO活性。

公开(公告)号：WO2011113798A3

公开(公告)日：2011-09-22

申请号：PCT/EP2011/053818

申请日：2011-03-14

Applicant: Proximagen Limited ,  EVANS, David ,  CARLEY, Allison ,  STEWART, Alison ,  HIGGINBOTTOM, Michael ,  SAVORY, Edward ,  SIMPSON, Iain ,  NILSSON, Marianne ,  HARALDSSON, Martin ,  NORDLING, Erik ,  KOOLMEISTER, Tobias

Inventor： EVANS, David ,  CARLEY, Allison ,  STEWART, Alison ,  HIGGINBOTTOM, Michael ,  SAVORY, Edward ,  SIMPSON, Iain ,  NILSSON, Marianne ,  HARALDSSON, Martin ,  NORDLING, Erik ,  KOOLMEISTER, Tobias

IPC: C07D471/04 ,  C07D487/04 ,  C07D498/08 ,  A61K31/437 ,  A61P35/00 ,  A61P37/06 ,  A61P11/08 ,  A61P25/28 ,  A61P9/10

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

公开(公告)号：WO2009102222A1

公开(公告)日：2009-08-20

申请号：PCT/NZ2009/000015

申请日：2009-02-13

Applicant: LINCOLN UNIVERSITY ,  STEWART, Alison

Inventor： STEWART, Alison

IPC: A01N63/04

CPC classification number: A01N63/04 ,  C12R1/885

Abstract: The present invention relates to Trichoderma atroviride strains and their use as biological control agents or plant growth promoters. Methods and compositions for biological control of soil borne plant pathogens, and increasing plant yield using T. atroviride are also provided.

Abstract translation: 本发明涉及叶绿体菌株及其作为生物防治剂或植物生长促进剂的用途。 还提供了用于生物防治土壤植物病原体的方法和组合物，以及使用阿特罗里韦提高植物产量。