公开(公告)号：WO2004081185A2

公开(公告)日：2004-09-23

申请号：PCT/US2004/007086

申请日：2004-03-08

Applicant: ATHENIX CORPORATION ,  BURDETTE, Jill ,  VANDE BERG, Brian ,  CARR, Brian ,  DUCK, Nicholas, B. ,  CAROZZI, Nadine ,  KOZIEL, Michael, G. ,  PATEL, Paresma, R.

Inventor： BURDETTE, Jill ,  VANDE BERG, Brian ,  CARR, Brian ,  DUCK, Nicholas, B. ,  CAROZZI, Nadine ,  KOZIEL, Michael, G. ,  PATEL, Paresma, R.

IPC: C12N

CPC classification number: C12P7/10 ,  C08H8/00 ,  C12N9/0006 ,  C12N9/18 ,  C12N9/20 ,  D21C5/005 ,  D21C9/16 ,  D21C11/0007 ,  Y02E50/16

Abstract: Methods for hydrolyzing lignocellulose are provided, comprising contacting the lignocellulose with at least one chemical treatment. Methods for pretreating a lignocellulosic material comprising contacting the material with at least one chemical are also provided. Methods for liberating a substance such as an enzyme, a pharmaceutical, or a nutraceutical from plant material are also provided. These methods are more efficient, more economical, and less toxic than current methods.

Abstract translation: 提供了用于水解木质纤维素的方法，包括使木质纤维素与至少一种化学处理物接触。 还提供了用于预处理木质纤维素材料的方法，包括使材料与至少一种化学品接触。 还提供了从植物材料中释放诸如酶，药物或营养制品的物质的方法。 这些方法比现有方法更高效，更经济，毒性更小。

公开(公告)号：WO2007008942A3

公开(公告)日：2007-04-12

申请号：PCT/US2006026976

申请日：2006-07-11

Applicant: AERIE PHARMACEUTICALS INC ,  DELONG MITCHELL A ,  SZNAIDMAN MARCOS L ,  OAKLEY ROBERT H ,  ECKHARDT ALLEN E ,  HUDSON CHRISTINE ,  YINGLING JEFFREY D ,  PEEL MICHAEL ,  RICHARDSON THOMAS E ,  MURRAY CLAIRE LOUISE ,  RAO BYAPPANAHALLY N NARASINGA ,  HEASLEY BRIAN H ,  PATEL PARESMA R

Inventor： DELONG MITCHELL A ,  SZNAIDMAN MARCOS L ,  OAKLEY ROBERT H ,  ECKHARDT ALLEN E ,  HUDSON CHRISTINE ,  YINGLING JEFFREY D ,  PEEL MICHAEL ,  RICHARDSON THOMAS E ,  MURRAY CLAIRE LOUISE ,  RAO BYAPPANAHALLY N NARASINGA ,  HEASLEY BRIAN H ,  PATEL PARESMA R

IPC: C07D213/61 ,  A61K31/341 ,  A61K31/381 ,  A61K31/4164 ,  A61K31/44 ,  A61K31/47 ,  A61K31/513 ,  A61P27/02 ,  C07C251/86 ,  C07D213/36 ,  C07D215/42 ,  C07D233/88 ,  C07D239/54 ,  C07D307/52 ,  C07D333/36

CPC classification number: C07D401/12 ,  C07D213/53 ,  C07D213/61 ,  C07D213/75 ,  C07D215/12 ,  C07D215/42 ,  C07D233/64 ,  C07D239/52 ,  C07D239/54 ,  C07D307/14 ,  C07D307/52 ,  C07D333/22 ,  C07D401/14

Abstract: Hydrazide compounds with GPCR desensitization inhibitory activity are provided that may be used to influence, inhibit or reduce the action of a G-protein receptor kinase. Pharmaceutical compositions including therapeutically effective amounts of the hydrazide compounds and pharmaceutically acceptable carriers are also provided. Various methods using the compounds and/or compositions to affect disease states or conditions controlled or influenced by GPCRs are also provided. Various methods using the compounds and/or compositions to affect disease states or conditions such as cancer osteoporosis and glaucoma are also provided. (Formula (I)). A is selected from a heteroaryl group (i): wherein X 1 , X 2 , X 3 and X 4 are, independently, CH, O, S or N-R 6 , with the proviso that at least one of X 2 or X 3 is O, S or N-R 6 ; and a heteroaryl group (ii): wherein X 5 and X 9 are CH or C-halogen, X 6 and X 8 are CH, and X 7 is N, and wherein the six-membered heteroaryl group may be further fused with an unsubstituted six-member aryl group; R 1 , R 2 , R 3 , R 4 , and R 5 are, independently, hydrogen; halogen; C 1 -C 4 alkyl; amino; nitro; cyano; heteroaryl; carboxy, carbonylamino; aminosulfonyl; sulfonylamino; aminoacyl; thioalkyl; sulfonyl; acyl; heterocycle; -OR; -O-C 1 -C 4 alkyl-heterocycle; -C(O)NH-C 1 -C 4 alkyl-heterocycle; -C(O)NH-heteroaryl; -C(O)NH-aryl; or carboxylamino; wherein R is C 1 -C 4 alkyl; aryl, heteroaryl, C 1 -C 4 alkyl aryl or C 1 -C 4 alkyl heteroaryl; R 6 is H or C 1 -C 4 alkyl; R 7 is hydrogen, C 1 -C 4 alkyl or C 1 -C 4 alkoxy; and X is N-R 6 .

Abstract translation: 提供具有GPCR脱敏抑制活性的酰肼化合物，其可用于影响，抑制或降低G蛋白受体激酶的作用。 还提供包含治疗有效量的酰肼化合物和药学上可接受的载体的药物组合物。 还提供了使用化合物和/或组合物影响受GPCR控制或影响的疾病状态或病症的各种方法。 还提供了使用化合物和/或组合物影响疾病状态或病症如癌症骨质疏松症和青光眼的各种方法。 （式（I））。 A选自杂芳基（i）：其中X 1，X 2，X 3和X 4 >独立地是CH，O，S或NR 6，条件是X 2或X 3中的至少一个是O ，S或NR 6; 和杂芳基（ii）：其中X 5和X 9是CH或C-卤素，X 6和X 8 H是CH，X 7是N，并且其中六元杂芳基可以进一步与未取代的六元芳基稠合; R 1，R 2，R 3，R 4和R 5， 独立地是氢; 卤素; C 1 -C 4烷基; 氨基; 硝基; 氰基; 杂; 羧基，羰基氨基; 氨基磺酰基; 磺酰; 氨; 硫代; 磺酰基; 酰基; 杂环; -要么; -O-C _{1 -C 4 烷基 - 杂环; -C（O）NH-C 1 -C 4 烷基 - 杂环; -C（O）NH杂芳基; -C（O）NH-芳基; 或羧基氨基; 其中R是C 1 -C 4烷基; 芳基，杂芳基，C 1 -C 4烷基芳基或C 1 -C 4烷基杂芳基; R 6是H或C 1 -C 4烷基; R 7是氢，C 1 -C 4烷基或C 1 -C 4烷基或C 1 -C 4 - 烷氧基; X为N-R 6。}

公开(公告)号：WO2004081185B1

公开(公告)日：2004-12-23

申请号：PCT/US2004007086

申请日：2004-03-08

Applicant: ATHENIX CORP ,  BURDETTE JILL ,  VANDE BERG BRIAN ,  CARR BRIAN ,  DUCK NICHOLAS B ,  CAROZZI NADINE ,  KOZIEL MICHAEL G ,  PATEL PARESMA R

Inventor： BURDETTE JILL ,  VANDE BERG BRIAN ,  CARR BRIAN ,  DUCK NICHOLAS B ,  CAROZZI NADINE ,  KOZIEL MICHAEL G ,  PATEL PARESMA R

IPC: C12N20060101 ,  C12N9/04 ,  C12N9/18 ,  C12N9/20 ,  C12P7/10 ,  C12P19/02 ,  C12S3/00 ,  C13K1/02 ,  D06M10/00

CPC classification number: C12P7/10 ,  C08H8/00 ,  C12N9/0006 ,  C12N9/18 ,  C12N9/20 ,  D21C5/005 ,  D21C9/16 ,  D21C11/0007 ,  Y02E50/16

Abstract: Methods for hydrolyzing lignocellulose are provided, comprising contacting the lignocellulose with at least one chemical treatment. Methods for pretreating a lignocellulosic material comprising contacting the material with at least one chemical are also provided. Methods for liberating a substance such as an enzyme, a pharmaceutical, or a nutraceutical from plant material are also provided. These methods are more efficient, more economical, and less toxic than current methods.

Abstract translation: 提供水解木质纤维素的方法，包括使木质纤维素与至少一种化学处理接触。 还提供了用于预处理木质纤维素材料的方法，包括使材料与至少一种化学品接触。 还提供了用于从植物材料释放诸如酶，药物或营养品的物质的方法。 这些方法比目前的方法更有效，更经济，毒性更低。

公开(公告)号：WO2007008942A2

公开(公告)日：2007-01-18

申请号：PCT/US2006/026976

申请日：2006-07-11

Applicant: AERIE PHARMACEUTICALS, INC. ,  DELONG, Mitchell, A. ,  SZNAIDMAN, Marcos, L. ,  OAKLEY, Robert, H. ,  ECKHARDT, Allen, E. ,  HUDSON, Christine ,  YINGLING, Jeffrey, D. ,  PEEL, Michael ,  RICHARDSON, Thomas, E. ,  MURRAY, Claire, Louise ,  RAO, Byappanahally, N. Narasinga ,  HEASLEY, Brian, H. ,  PATEL, Paresma, R.

Inventor： DELONG, Mitchell, A. ,  SZNAIDMAN, Marcos, L. ,  OAKLEY, Robert, H. ,  ECKHARDT, Allen, E. ,  HUDSON, Christine ,  YINGLING, Jeffrey, D. ,  PEEL, Michael ,  RICHARDSON, Thomas, E. ,  MURRAY, Claire, Louise ,  RAO, Byappanahally, N. Narasinga ,  HEASLEY, Brian, H. ,  PATEL, Paresma, R.

CPC classification number: C07D401/12 ,  C07D213/53 ,  C07D213/61 ,  C07D213/75 ,  C07D215/12 ,  C07D215/42 ,  C07D233/64 ,  C07D239/52 ,  C07D239/54 ,  C07D307/14 ,  C07D307/52 ,  C07D333/22 ,  C07D401/14

Abstract: Hydrazide compounds with GPCR desensitization inhibitory activity are provided that may be used to influence, inhibit or reduce the action of a G-protein receptor kinase. Pharmaceutical compositions including therapeutically effective amounts of the hydrazide compounds and pharmaceutically acceptable carriers are also provided. Various methods using the compounds and/or compositions to affect disease states or conditions controlled or influenced by GPCRs are also provided. Various methods using the compounds and/or compositions to affect disease states or conditions such as cancer, osteoporosis and glaucoma are also provided.

Abstract translation: 提供具有GPCR脱敏抑制活性的酰肼化合物，其可用于影响，抑制或降低G蛋白受体激酶的作用。 还提供包含治疗有效量的酰肼化合物和药学上可接受的载体的药物组合物。 还提供了使用化合物和/或组合物影响受GPCR控制或影响的疾病状态或病症的各种方法。 还提供了使用化合物和/或组合物影响疾病状态或病症如癌症，骨质疏松症和青光眼的各种方法。

公开(公告)号：WO2016011019A1

公开(公告)日：2016-01-21

申请号：PCT/US2015/040366

申请日：2015-07-14

Applicant: THE BRIGHAM AND WOMEN'S HOSPITAL, INC. ,  THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES ,  LEE, Arthur ,  MCKEW, John, C. ,  PATEL, Paresma, R. ,  YU, Paul, B. ,  MOHEDAS, Agustin, H. ,  SANDERSON, Philip, E. ,  ZHENG, Wei ,  HUANG, Xiuli ,  UNIVERSITY OF HOUSTON SYSTEM

Inventor： LEE, Arthur ,  MCKEW, John, C. ,  PATEL, Paresma, R. ,  YU, Paul, B. ,  MOHEDAS, Agustin, H. ,  SANDERSON, Philip, E. ,  ZHENG, Wei ,  HUANG, Xiuli ,  CUNY, Gregory, D.

IPC: C07D487/04 ,  A61K31/519 ,  A61P9/00 ,  A61P3/06 ,  A61P29/00 ,  A61P31/00 ,  A61P35/00 ,  A61P33/00 ,  A61K31/53 ,  A61P21/00

CPC classification number: C07D487/04 ,  C07D519/00

Abstract: The present invention provides small-molecule inhibitors of BMP signaling and compositions and methods for inhibiting BMP signaling. These compounds and compositions may be used to modulate cell growth, differentiation, proliferation, and apoptosis, and thus may be useful for treating diseases or conditions associated with BMP signaling, including inflammation, cardiovascular disease, hematological disease, cancer, and bone disorders, as well as for modulating cellular differentiation and/or proliferation. These compounds and compositions may also be used to reduce circulating levels of ApoB-100 or LDL and treat or prevent acquired or congenital hypercholesterolemia or hyperlipoproteinemia; diseases, disorders, or syndromes associated with defects in lipid absorption or metabolism; or diseases, disorders, or syndromes caused by hyperlipidemia.

Abstract translation: 本发明提供了BMP信号的小分子抑制剂以及用于抑制BMP信号传导的组合物和方法。 这些化合物和组合物可用于调节细胞生长，分化，增殖和凋亡，因此可用于治疗与BMP信号相关的疾病或病症，包括炎症，心血管疾病，血液病，癌症和骨骼疾病，如 以及调节细胞分化和/或增殖。 这些化合物和组合物也可用于降低ApoB-100或LDL的循环水平并治疗或预防获得性或先天性高胆固醇血症或高脂蛋白血症; 与脂质吸收或代谢缺陷相关的疾病，病症或综合征; 或由高脂血症引起的疾病，病症或综合征。

公开(公告)号：WO2007008926A1

公开(公告)日：2007-01-18

申请号：PCT/US2006/026947

申请日：2006-07-11

Applicant: AERIE PHARMACEUTICALS, INC. ,  DELONG, Mitchell, A. ,  SZNAIDMAN, Marcos, L. ,  OAKLEY, Robert, H. ,  ECKHARDT, Allen, E. ,  HUDSON, Christine ,  YINGLING, Jeffrey, D. ,  PEEL, Michael ,  RICHARDSON, Thomas, E. ,  MURRAY, Claire, Louise ,  RAO, Byappanahally N., Narasinga ,  HEASLEY, Brian, H. ,  PATEL, Paresma, R.

Inventor： DELONG, Mitchell, A. ,  SZNAIDMAN, Marcos, L. ,  OAKLEY, Robert, H. ,  ECKHARDT, Allen, E. ,  HUDSON, Christine ,  YINGLING, Jeffrey, D. ,  PEEL, Michael ,  RICHARDSON, Thomas, E. ,  MURRAY, Claire, Louise ,  RAO, Byappanahally N., Narasinga ,  HEASLEY, Brian, H. ,  PATEL, Paresma, R.

IPC: C07D217/02 ,  A61K31/472 ,  A61P27/06

CPC classification number: C07D217/02

Abstract: Isoquinoline compounds are provided that influence, inhibit or reduce the action of a G-protein receptor kinase . Pharmaceutical compositions including therapeutically effective amounts of the isoquinoline compounds and pharmaceutically acceptable carriers are also provided. Various methods using the compounds and/or compositions to affect disease states or conditions such as cancer, osteoporosis and glaucoma are also provided.

Abstract translation: 提供了影响，抑制或降低G蛋白受体激酶作用的异喹啉化合物。 还提供包含治疗有效量的异喹啉化合物和药学上可接受的载体的药物组合物。 还提供了使用化合物和/或组合物影响疾病状态或病症如癌症，骨质疏松症和青光眼的各种方法。

公开(公告)号：WO2004081185A3

公开(公告)日：2004-10-21

申请号：PCT/US2004007086

申请日：2004-03-08

Applicant: ATHENIX CORP ,  BURDETTE JILL ,  VANDE BERG BRIAN ,  CARR BRIAN ,  DUCK NICHOLAS B ,  CAROZZI NADINE ,  KOZIEL MICHAEL G ,  PATEL PARESMA R

Inventor： BURDETTE JILL ,  VANDE BERG BRIAN ,  CARR BRIAN ,  DUCK NICHOLAS B ,  CAROZZI NADINE ,  KOZIEL MICHAEL G ,  PATEL PARESMA R

IPC: C12N20060101 ,  C12N9/04 ,  C12N9/18 ,  C12N9/20 ,  C12P7/10 ,  C12P19/02 ,  C12S3/00 ,  C13K1/02 ,  D06M10/00

CPC classification number: C12P7/10 ,  C08H8/00 ,  C12N9/0006 ,  C12N9/18 ,  C12N9/20 ,  D21C5/005 ,  D21C9/16 ,  D21C11/0007 ,  Y02E50/16

Abstract: Methods for hydrolyzing lignocellulose are provided, comprising contacting the lignocellulose with at least one chemical treatment. Methods for pretreating a lignocellulosic material comprising contacting the material with at least one chemical are also provided. Methods for liberating a substance such as an enzyme, a pharmaceutical, or a nutraceutical from plant material are also provided. These methods are more efficient, more economical, and less toxic than current methods.

Abstract translation: 提供了用于水解木质纤维素的方法，包括使木质纤维素与至少一种化学处理剂接触。 还提供了用于预处理木质纤维素材料的方法，包括使材料与至少一种化学品接触。 还提供了从植物材料中释放诸如酶，药物或营养制品的物质的方法。 这些方法比现有方法更高效，更经济，毒性更小。