公开(公告)号：WO2010032009A1

公开(公告)日：2010-03-25

申请号：PCT/GB2009/002221

申请日：2009-09-18

申请人： PIMCO 2664 Limited ,  GREIG, Iain Robert ,  SHERIDAN, Rose Mary ,  FISHER, Raymond ,  TOZER, Matthew, John ,  CLASE, Juha, Andrew ,  SMITH, Andrew ,  TUFFNELL, Andrew, Robert ,  VAN 'T HOF, Robert, Jurgen

发明人： GREIG, Iain Robert ,  SHERIDAN, Rose Mary ,  FISHER, Raymond ,  TOZER, Matthew, John ,  CLASE, Juha, Andrew ,  SMITH, Andrew ,  TUFFNELL, Andrew, Robert ,  VAN 'T HOF, Robert, Jurgen

IPC分类号： C07C311/20 ,  C07C311/28 ,  C07D213/52 ,  C07D239/26 ,  C07D239/30 ,  C07D295/135 ,  A61K31/18 ,  A61P29/00

CPC分类号： A61K31/18 ,  A61K31/44 ,  A61K31/4418 ,  A61K31/505 ,  C07C311/20 ,  C07C311/28 ,  C07C311/29 ,  C07D207/04 ,  C07D213/34 ,  C07D213/52 ,  C07D213/61 ,  C07D239/26 ,  C07D239/30 ,  C07D295/135

摘要： The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain aryl-phenyl-sulfonamido-cycloalkyl compounds of the following formula (collectively referred to herein as "APSAC compounds"). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, in treatment, for example, of inflammation and/or joint destruction and/or bone loss; of disorders mediated by excessive and/or inappropriate and/or prolonged activation of the immune system; of inflammatory and autoimmune disorders, for example, rheumatoid arthritis, psoriasis, psoriatic arthritis, chronic obstructive pulmonary disease (COPD), atherosclerosis, inflammatory bowel disease, ankylosing spondylitis, and the like; of disorders associated with bone loss, such as bone loss associated with excessive osteoclast activity in rheumatoid arthritis, osteoporosis, cancer-associated bone disease, Paget's disease and the like, etc.; and of cancer, such as a haematological malignancy, a solid tumour, etc. Formula (I).

摘要翻译： 本发明一般涉及治疗化合物领域，更具体地涉及下列通式的某些芳基 - 苯基 - 亚磺酰氨基 - 环烷基化合物（在本文中统称为“APSAC化合物”）。 本发明还涉及包含这些化合物的药物组合物，以及体外和体内的这些化合物和组合物在治疗例如炎症和/或关节破坏和/或骨丢失中的用途; 由免疫系统的过度和/或不适当和/或延长的激活介导的疾病; 炎性和自身免疫性疾病，例如类风湿性关节炎，牛皮癣，牛皮癣关节炎，慢性阻塞性肺病（COPD），动脉粥样硬化，炎性肠病，强直性脊柱炎等; 与骨丢失相关的疾病，例如与类风湿性关节炎中的过度破骨细胞活性相关的骨丢失，骨质疏松症，癌症相关的骨病，佩吉特氏病等; 和癌症，如血液恶性肿瘤，实体肿瘤等。式（I）。

公开(公告)号：WO2008114022A1

公开(公告)日：2008-09-25

申请号：PCT/GB2008/000989

申请日：2008-03-20

申请人： THE UNIVERSITY COURT OF THE UNIVERSITY OF ABERDEEN ,  GREIG, Iain, Robert ,  VAN 'T HOF, Robert, Jurgen ,  RALSTON, Stuart, Hamilton

发明人： GREIG, Iain, Robert ,  VAN 'T HOF, Robert, Jurgen ,  RALSTON, Stuart, Hamilton

IPC分类号： C07C311/21 ,  A61K31/18 ,  A61P17/06 ,  A61P19/00 ,  A61P19/02 ,  A61P19/08 ,  A61P29/00

CPC分类号： C07C311/21 ,  C07C311/44 ,  C07C311/46 ,  C07C317/14

摘要： The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain aryl sulfonamides and related compounds (collectively referred to herein as "BPSAAA compounds"), as described herein, and including, for example, biphenyl-4-sulfonic acid (hydroxyalkyl-phenyl)-amides and related compounds. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo , in treatment and/or prevention, for example, of inflammation and/or joint destruction and/or bone loss; of disorders mediated by excessive and/or inappropriate and/or prolonged activation of the immune system; of, inflammatory and autoimmune disorders, for example, rheumatoid arthritis, psoriasis, psoriatic arthritis, chronic obstructive pulmonary disease (COPD), atherosclerosis, inflammatory bowel disease, ankylosing spondylitis, and the like; of disorders associated with bone loss, such as bone loss associated with excessive osteoclast activation in rheumatoid arthritis, osteoporosis, cancer associated bone disease, Paget's disease and the like.

摘要翻译： 本发明一般涉及治疗化合物领域，更具体地涉及某些芳基磺酰胺和相关化合物（本文统称为“BPSAAA化合物”），如本文所述，并且包括例如联苯-4-磺酸 （羟基烷基 - 苯基） - 酰胺和相关化合物。 本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在体外和体内在治疗和/或预防例如炎症和/或关节破坏和/或骨丢失中的用途 ; 由免疫系统的过度和/或不适当和/或延长的激活介导的疾病; 的炎性和自身免疫性疾病，例如类风湿性关节炎，牛皮癣，银屑病关节炎，慢性阻塞性肺病（COPD），动脉粥样硬化，炎性肠病，强直性脊柱炎等; 与骨丢失相关的疾病，例如与类风湿性关节炎中的过度破骨细胞活化相关的骨丢失，骨质疏松症，癌症相关的骨病，佩吉特氏病等。

公开(公告)号：WO2004098582A2

公开(公告)日：2004-11-18

申请号：PCT/GB2004/001958

申请日：2004-05-06

申请人： THE UNIVERSITY COURT OF THE UNIVERSITY OF ABERDEEN ,  RALSTON, Stuart, Hamilton ,  GREIG, Iain, Robert ,  MOHAMED, Aymen, Ibrahim, Idris ,  VAN'T HOF, Robert, Jurgen

发明人： RALSTON, Stuart, Hamilton ,  GREIG, Iain, Robert ,  MOHAMED, Aymen, Ibrahim, Idris ,  VAN'T HOF, Robert, Jurgen

IPC分类号： A61K31/12

CPC分类号： C07C43/315 ,  A61K31/12 ,  A61K31/403 ,  C07C33/26 ,  C07C33/36 ,  C07C33/38 ,  C07C33/46 ,  C07C33/486 ,  C07C43/1782 ,  C07C45/004 ,  C07C45/46 ,  C07C45/567 ,  C07C45/673 ,  C07C49/784 ,  C07C49/796 ,  C07C49/813 ,  C07C59/84 ,  C07C69/007 ,  C07C205/19 ,  C07C205/45 ,  C07C251/48 ,  C07C259/10 ,  C07C2603/18 ,  C07C2603/26 ,  C07D309/12 ,  C07D339/08 ,  C07C49/84 ,  C07C49/83

摘要： The present invention pertains to certain ketones and reduced ketones and derivatives thereof which, inter alia , inhibit osteoclast survival, formation, and/or activity; and/or inhibit bone resorption, and more particularly to compounds of the formulae: (1) (2) wherein: Ar 1 is independently a biphenyl, phenanthryl, fluorenyl, or carbazolyl, and is optionally substituted; R alk is independently a C 2-10 alkylene group, and is optionally substituted; -OR O , if present, is independently -OH or -OR K ; -OR K , if present, is independently selected from: -O-R K1 ; -O-C(=O)R K2 ; -O-C(=O)OR K3 ; -O-S(=O)2OR K4 ; Q is independently -OH or -OR OT ; wherein: -OR OT , if present, is independently selected from: -O-R E1 ; -O-C(=O)-R E2 ; -O-C(=O)-O-R E3 ; -O-C(=O)-O-SO 3 R E4 ; -O-C(=O)-O-(CH 2 ) n -COOR E5 ; -O-C(=O)-(CH 2 ) n -NR N1 R N2 ; -O-C(=O)-(CH 2 ) n -NH-C(=O)R E6 ; -O-C(=O)-(CH 2 ) n -C(=O)-NR N3 R N4 ; -O-P(=O)(OR E7 )(OR E8 ); -O-R PA ; R PA , if present, is an organic group which incorporates a phosphonic acid group; with the proviso that if -OR OT is -O-R E1 , then R E1 is not a phenyl group substituted with a sulfonyl group; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, chemically protected forms, or prodrugs thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo , to inhibit osteoclast survival, formation, and/or activity, and to inhibit conditions mediated by osteoclasts and/or characterised by bone resorption, in the treatment of bone disorders such as osteoporosis, rheumatoid arthritis, cancer associated bone disease, Paget's disease, aseptic loosening of prosthetic implants, and the like; and/or in the treatment of conditions associated with inflammation or activation of the immune system.

摘要翻译： 本发明涉及某些酮和还原酮及其衍生物，其特别是抑制破骨细胞存活，形成和/或活性; 尤其涉及下式的化合物：（1）（2）其中：Ar 1独立地是联苯基，菲基，芴基或咔唑基，并且任选被取代; R a烷基独立地为C 2-10亚烷基，并且任选被取代; -ORO，如果存在，独立地是-OH或-ORK; -OR ，如果存在，独立地选自：-O-R ; -O-C（= O）R ; -O-C（= O）OR ; -O-S（= O）2 OR ; Q独立地为-OH或-ORO; 其中：-OR OT如果存在，独立地选自：-O-R E1; -O-C（= O）-R ; -O-C（= O）-O-R ; -O-C（= O）-O-SO 3 ; -O-C（= O）-O-（CH 2）N-COOR ; -O-C（= O） - （CH 2）N-NR - [R ; -O-C（= O） - （CH 2）N-NH-C（= O）R ; -O-C（= O） - （CH 2）N-C（= O）-NR - [R ; -O-P（= O）（OR ）（OR ）; -O-R ; 如果存在，R PA是含有膦酸基的有机基团; 条件是如果-OR OT是-O-R ，则R E1不是被磺酰基取代的苯基; 和其药学上可接受的盐，溶剂合物，酰胺，酯，醚，化学保护形式或前药。 本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在体外和体内的用途，以抑制破骨细胞存活，形成和/或活性，以及​​抑制破骨细胞介导的病症和/或 其特征在于骨吸收，治疗诸如骨质疏松症，类风湿性关节炎，癌症相关骨病，佩吉特氏病，假体植入物的无菌性松动等骨骼疾病; 和/或治疗与炎症或免疫系统的激活相关的病症。

公开(公告)号：WO2004078261A1

公开(公告)日：2004-09-16

申请号：PCT/GB2004/000858

申请日：2004-03-02

申请人： THE UNIVERSITY COURT OF THE UNIVERSITY OF ABERDEEN ,  RALSTON, Stuart, Hamilton ,  GREIG, Iain, Robert ,  ROSS, Ruth, Alexandra ,  MOHAMED, Aymen, Ibrahim, Idris ,  VAN'T HOF, Robert, Jurgen

发明人： RALSTON, Stuart, Hamilton ,  GREIG, Iain, Robert ,  ROSS, Ruth, Alexandra ,  MOHAMED, Aymen, Ibrahim, Idris ,  VAN'T HOF, Robert, Jurgen

IPC分类号： A61P19/08

CPC分类号： A61K31/415 ,  A61K31/454 ,  A61K31/4709 ,  A61K31/5377

摘要： The present invention pertains to cannabinoid (CB) receptor inverse agonists and neutral antagonists, and especially CB1 and CB2 inverse agonists and neutral antagonists; such as, for example, certain pyrazole compounds; their use in the inhibition of osteoclasts (for example, the inhibition of the survival, formation, and/or activity of osteoclasts), and/or in the inhibition of bone resorption; their use in connection with treatment of bone disorders, such as conditions mediated by osteoclasts (e.g., increased osteoclast activity) and/or characterised by (e.g., increased) bone resorption, such as osteoporosis (e.g., osteoporosis not associated with inflammation; e.g., osteoporosis associated with a genetic predisposition, sex hormone deficiency, or ageing), cancer associated bone disease, and Paget's disease of bone.

摘要翻译： 本发明涉及大麻素（CB）受体反向激动剂和中性拮抗剂，特别是CB1和CB2反向激动剂和中性拮抗剂; 例如，某些吡唑化合物; 它们在抑制破骨细胞中的用途（例如，抑制破骨细胞的存活，形成和/或活性）和/或抑制骨吸收; 其用于治疗骨骼疾病，例如由破骨细胞介导的病症（例如增加的破骨细胞活性）和/或特征在于（例如，增加的）骨吸收，例如骨质疏松症（例如，与炎症无关的骨质疏松症） 与遗传易感性相关的骨质疏松症，性激素缺乏或衰老），癌症相关的骨病和骨的佩吉特氏病。

公开(公告)号：WO2004098582A3

公开(公告)日：2005-04-21

申请号：PCT/GB2004001958

申请日：2004-05-06

申请人： UNIV ABERDEEN ,  RALSTON STUART HAMILTON ,  GREIG IAIN ROBERT ,  MOHAMED AYMEN IBRAHIM IDRIS ,  VAN T HOF ROBERT JURGEN

发明人： RALSTON STUART HAMILTON ,  GREIG IAIN ROBERT ,  MOHAMED AYMEN IBRAHIM IDRIS ,  VAN T HOF ROBERT JURGEN

IPC分类号： A61K31/12 ,  A61K31/403 ,  A61P19/02 ,  A61P19/08 ,  A61P19/10 ,  C07C33/26 ,  C07C33/36 ,  C07C33/38 ,  C07C33/46 ,  C07C33/48 ,  C07C43/178 ,  C07C43/315 ,  C07C45/00 ,  C07C45/46 ,  C07C45/56 ,  C07C45/67 ,  C07C49/784 ,  C07C49/796 ,  C07C49/813 ,  C07C59/84 ,  C07C69/007 ,  C07C205/19 ,  C07C205/45 ,  C07C251/48 ,  C07C259/10 ,  C07D309/12 ,  C07D339/08 ,  C07C33/34 ,  C07C49/215 ,  C07D209/86

CPC分类号： C07C43/315 ,  A61K31/12 ,  A61K31/403 ,  C07C33/26 ,  C07C33/36 ,  C07C33/38 ,  C07C33/46 ,  C07C33/486 ,  C07C43/1782 ,  C07C45/004 ,  C07C45/46 ,  C07C45/567 ,  C07C45/673 ,  C07C49/784 ,  C07C49/796 ,  C07C49/813 ,  C07C59/84 ,  C07C69/007 ,  C07C205/19 ,  C07C205/45 ,  C07C251/48 ,  C07C259/10 ,  C07C2603/18 ,  C07C2603/26 ,  C07D309/12 ,  C07D339/08 ,  C07C49/84 ,  C07C49/83

摘要： The present invention pertains to certain ketones and reduced ketones and derivatives thereof which, inter alia, inhibit osteoclast survival, formation, and/or activity; and/or inhibit bone resorption, and more particularly to compounds of the formulae: (1) (2) wherein: Ar is independently a biphenyl, phenanthryl, fluorenyl, or carbazolyl, and is optionally substituted; R is independently a C2-10alkylene group, and is optionally substituted; -OR , if present, is independently -OH or -OR ; -OR , if present, is independently selected from: -O-R ; -O-C(=O)R ; -O-C(=O)OR ; -O-S(=O)2OR ; Q is independently -OH or -OR ; wherein: -OR , if present, is independently selected from: -O-R ; -O-C(=O)-R ; -O-C(=O)-O-R ; -O-C(=O)-O-SO3R ; -O-C(=O)-O-(CH2)n-COOR ; -O-C(=O)-(CH2)n-NR R ; -O-C(=O)-(CH2)n-NH-C(=O)R ; -O-C(=O)-(CH2)n-C(=O)-NR R ; -O-P(=O)(OR )(OR ); -O-R ; R , if present, is an organic group which incorporates a phosphonic acid group; with the proviso that if -OR is -O-R , then R is not a phenyl group substituted with a sulfonyl group; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, chemically protected forms, or prodrugs thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit osteoclast survival, formation, and/or activity, and to inhibit conditions mediated by osteoclasts and/or characterised by bone resorption, in the treatment of bone disorders such as osteoporosis, rheumatoid arthritis, cancer associated bone disease, Paget's disease, aseptic loosening of prosthetic implants, and the like; and/or in the treatment of conditions associated with inflammation or activation of the immune system.

摘要翻译： 本发明涉及某些酮和还原酮及其衍生物，其特别是抑制破骨细胞存活，形成和/或活性; 尤其涉及下式的化合物：（1）（2）其中：Ar 1独立地是联苯基，菲基，芴基或咔唑基，并且是任选被取代的; R a烷基独立地为C 2-10亚烷基，并且任选被取代; -ORO，如果存在，独立地是-OH或-ORK; -OR ，如果存在，独立地选自：-O-R ; -O-C（= O）R ; -O-C（= O）OR ; -O-S（= O）2 OR ; Q独立地为-OH或-ORO; 其中：-OR OT如果存在，独立地选自：-O-R E1; -O-C（= O）-R ; -O-C（= O）-O-R ; -O-C（= O）-O-SO 3 ; -O-C（= O）-O-（CH 2）N-COOR ; -O-C（= O） - （CH 2）N-NR - [R ; -O-C（= O） - （CH 2）N-NH-C（= O）R ; -O-C（= O） - （CH 2）N-C（= O）-NR - [R ; -O-P（= O）（OR ）（OR ）; -O-R ; 如果存在，R PA是含有膦酸基的有机基团; 条件是如果-OR OT是-O-R ，则R E1不是被磺酰基取代的苯基; 和其药学上可接受的盐，溶剂合物，酰胺，酯，醚，化学保护形式或前药。 本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在体外和体内的用途，以抑制破骨细胞存活，形成和/或活性，以及​​抑制破骨细胞介导的病症和/或 其特征在于骨吸收，治疗诸如骨质疏松症，类风湿性关节炎，癌症相关骨病，佩吉特氏病，假体植入物的无菌性松动等骨骼疾病; 和/或治疗与炎症或免疫系统的激活相关的病症。

公开(公告)号：WO1998020015A1

公开(公告)日：1998-05-14

申请号：PCT/GB1997003034

申请日：1997-11-04

申请人： THE UNIVERSITY COURT OF THE UNIVERSITY OF ST ANDREWS ,  BUTLER, Anthony, Robert ,  GREIG, Iain, Robert ,  MEGSON, Ian, Lennox

发明人： THE UNIVERSITY COURT OF THE UNIVERSITY OF ST ANDREWS

IPC分类号： C07H03/04

CPC分类号： C07H3/06 ,  A61K9/0019 ,  A61K9/7023 ,  C07H3/04

摘要： Disclosed is a compound capable of releasing nitric oxide from an S-nitrosothiol group (-S-N=O), the compound comprising an S-nitrosothiol group linked via an intervening moiety, to a mono-, di- or trisaccharide moiety, wherein the mono-, di- or trisaccharide moiety may be fully substituted, partially substituted, or unsubstituted, and wherein the intervening moiety serves to stabilise the S-nitrosothiol group to prevent rapid degradation thereof; together with a method of making the compound, a composition comprising the compound, and a method of causing smooth muscle relaxation.

摘要翻译： 公开了一种能够从S-亚硝基硫醇基团（-SN = O）释放一氧化氮的化合物，其包含通过中间部分连接的S-亚硝基硫醇基团的单体，二糖或三糖部分，其中单 - - ，二 - 或三糖部分可以是完全取代的，部分取代的或未取代的，并且其中所述中间部分用于稳定S-亚硝基硫醇基团以防止其快速降解; 以及制备该化合物的方法，包含该化合物的组合物和引起平滑肌松弛的方法。

公开(公告)号：WO2008099139A1

公开(公告)日：2008-08-21

申请号：PCT/GB2008/000435

申请日：2008-02-07

申请人： THE UNIVERSITY COURT OF THE UNIVERSITY OF ABERDEEN ,  GREIG, Iain, Robert ,  ROSS, Ruth, Alexandra ,  PERTWEE, Roger, Guy

发明人： GREIG, Iain, Robert ,  ROSS, Ruth, Alexandra ,  PERTWEE, Roger, Guy

IPC分类号： C07D231/12 ,  A61K31/415 ,  A61P29/00

CPC分类号： C07D231/12

摘要： The present invention pertains to cannabinoid (CB) receptor neutral antagonists, and especially CB1 neutral antagonists, and including, for example, certain 1,5-di-aryl-pyrazole compounds. The present invention also pertains to the use of such compounds in the treatment of diseases and disorders that are ameliorated by treatment with a neutral antagonist of the cannabinoid type 1 (CB1) receptor, for example: an eating disorder; obesity; a disease or disorder characterised by an addiction component; addiction; withdrawal; smoking addiction; smoking withdrawal; drug addiction; drug withdrawal; smoking cessation therapy; a bone disease or disorder; osteoporosis, Paget's disease of bone; bone related cancer; a disease or disorder with an inflammatory or autoimmune component; rheumatoid arthritis; inflammatory bowel disease; psoriasis; a psychiatric disease or disorder; anxiety; mania; schizophrenia; a disease or disorder characterised by impairment of memory and/or loss of cognitive function; memory impairment; loss of cognitive function; Parkinson's disease; Alzheimer's disease; dementia; a cardiovascular disease or disorder; congestive heart failure; cardiac hypertrophy; and myocardial infarction.

摘要翻译： 本发明涉及大麻素（CB）受体中性拮抗剂，特别是CB1中性拮抗剂，并且包括例如某些1,5-二芳基吡唑化合物。 本发明还涉及这种化合物在治疗通过用大麻素1型（CB1）受体的中性拮抗剂治疗而改善的疾病和病症的用途，例如：进食障碍; 肥胖; 以成瘾成分为特征的疾病或病症; 瘾; 退出; 吸烟成瘾; 戒烟 药物成瘾; 戒毒 戒烟治疗 骨病或病症; 骨质疏松症，佩吉特氏骨病; 骨相关癌症; 具有炎性或自身免疫组分的疾病或病症; 类风湿关节炎; 炎症性肠病; 银屑病; 精神疾病或病症; 焦虑; 狂躁; 精神分裂症; 以记忆障碍和/或认知功能丧失为特征的疾病或病症; 记忆障碍 认知功能丧失; 帕金森病 阿尔茨海默氏病; 痴呆; 心血管疾病或病症; 充血性心力衰竭; 心脏肥大; 和心肌梗塞。

公开(公告)号：WO2013038153A1

公开(公告)日：2013-03-21

申请号：PCT/GB2012/052206

申请日：2012-09-07

申请人： THE UNIVERSITY COURT OF THE UNIVERSITY OF ABERDEEN ,  ZANDA, Matteo ,  PLATT, Bettina ,  GREIG, Iain Robert ,  CALAMAI, Elisa

发明人： ZANDA, Matteo ,  PLATT, Bettina ,  GREIG, Iain Robert ,  CALAMAI, Elisa

IPC分类号： C07D239/04 ,  C07B59/00 ,  G01T1/161 ,  A61K51/04 ,  C07D239/62 ,  C07D239/66

CPC分类号： C07D239/62 ,  C07B59/002 ,  C07D239/66

摘要： The present invention relates generally to the field of diagnostic methods. More specifically, the present invention pertains to certain 18F-labelled barbiturate compounds of the following formula (collectively referred to herein as "18F-fluorinated barbiturate compounds" and "18FBAR compounds") that bind to metals, for example, metals associated with protein aggregates, and as such are useful as imaging agents for positron emission imaging (e.g., positron emission tomography (PET) imaging) used in the diagnosis and monitoring of conditions involving these aggregates, including Alzheimer's disease (AD), Parkinson's disease (PD), and Huntington's disease (HD). These compounds also bind strongly to GABAA receptors and hence are also useful as imaging agents for positron emission tomography (PET) imaging used in the diagnosis, monitoring and study of diseases involving dis-regulation of these receptors, including epilepsy, schizophrenia, and mood disorders (e.g., anxiety).

摘要翻译： 本发明一般涉及诊断方法领域。 更具体地说，本发明涉及与金属例如与蛋白质聚集体相关的金属的某些18F标记的巴比妥类化合物（以下统称为“18F-氟化巴比妥酸盐化合物”和“18FBAR化合物”）） 并且因此可用作用于诊断和监测涉及这些聚集物的病症（包括阿尔茨海默氏病（AD）），帕金森病（PD）和正常发射成像（PET））的正电子发射成像（例如，正电子发射断层摄影（PET）成像） 亨廷顿病（HD）。 这些化合物也与GABA A受体强烈结合，因此也可用作用于诊断，监测和研究涉及这些受体包括癫痫，精神分裂症和情绪障碍的疾病的疾病的正电子发射断层摄影（PET）成像的成像剂。 （例如，焦虑）。

公开(公告)号：WO2010032010A1

公开(公告)日：2010-03-25

申请号：PCT/GB2009/002223

申请日：2009-09-18

申请人： PIMCO 2664 LIMITED ,  GREIG, Iain, Robert ,  SHERIDAN, Rose, Mary ,  FISHER, Raymond ,  TOZER, Matthew, John ,  CLASE, Juha, Andrew ,  SMITH, Andrew ,  TUFFNELL, Andrew, Robert ,  VAN 'T HOF, Robert, Jurgen

发明人： GREIG, Iain, Robert ,  SHERIDAN, Rose, Mary ,  FISHER, Raymond ,  TOZER, Matthew, John ,  CLASE, Juha, Andrew ,  SMITH, Andrew ,  TUFFNELL, Andrew, Robert ,  VAN 'T HOF, Robert, Jurgen

IPC分类号： C07C311/21 ,  C07D295/135 ,  A61K31/18 ,  A61P19/00 ,  A61P19/02 ,  A61P19/08 ,  A61P19/10 ,  A61P29/00 ,  A61P35/00

CPC分类号： C07D303/36 ,  C07C311/21 ,  C07C311/39 ,  C07C2601/02 ,  C07D239/26 ,  C07D239/30 ,  C07D263/20 ,  C07D295/135

摘要： The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain aryl-phenyl-sulfonamido-phenylene compounds of the following formula (I) (collectively referred to herein as "APSAP compounds"). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, in treatment, for example, of inflammation and/or joint destruction and/or bone loss; of disorders mediated by excessive and/or inappropriate and/or prolonged activation of the immune system; of inflammatory and autoimmune disorders, for example, rheumatoid arthritis, psoriasis, psoriatic arthritis, chronic obstructive pulmonary disease (COPD), atherosclerosis, inflammatory bowel disease, ankylosing spondylitis, and the like; of disorders associated with bone loss, such as bone loss associated with excessive osteoclast activity in rheumatoid arthritis, osteoporosis, cancer-associated bone disease, Paget's disease and the like, etc.; and of cancer, such as a haematological malignancy, a solid tumour, etc.

摘要翻译： 本发明一般涉及治疗化合物领域，更具体地涉及下列通式（I）的某些芳基 - 苯基 - 亚磺酰氨基 - 亚苯基化合物（本文统称为“APSAP化合物”）。 本发明还涉及包含这些化合物的药物组合物，以及体外和体内的这些化合物和组合物在治疗例如炎症和/或关节破坏和/或骨丢失中的用途; 由免疫系统的过度和/或不适当和/或延长的激活介导的疾病; 炎性和自身免疫性疾病，例如类风湿性关节炎，牛皮癣，牛皮癣关节炎，慢性阻塞性肺病（COPD），动脉粥样硬化，炎性肠病，强直性脊柱炎等; 与骨丢失相关的疾病，例如与类风湿性关节炎中的过度破骨细胞活性相关的骨丢失，骨质疏松症，癌症相关的骨病，佩吉特氏病等; 和癌症，如血液恶性肿瘤，实体瘤等。

公开(公告)号：WO2010020762A1

公开(公告)日：2010-02-25

申请号：PCT/GB2009/001999

申请日：2009-08-14

申请人： THE UNIVERSITY COURT OF THE UNIVERSITY OF ABERDEEN ,  GREIG, Iain, Robert ,  ROSS, Ruth, Alexandra

发明人： GREIG, Iain, Robert ,  ROSS, Ruth, Alexandra

IPC分类号： C07D401/06 ,  C07D403/06 ,  A61K31/4439 ,  A61K31/506 ,  A61P3/00 ,  A61P9/00 ,  A61P19/00 ,  A61P25/00 ,  A61P35/00 ,  A61P29/00

CPC分类号： C07D403/06 ,  C07D401/06

摘要： The present invention pertains to cannabinoid (CB) receptor and cannabinoid-like receptor neutral antagonists, and especially CB1 neutral antagonists of Formula (I). The present invention also pertains to these compounds for use in the treatment of diseases and disorders that are ameliorated by treatment with a neutral antagonist of the cannabinoid type 1 (CB1) receptor or a non-CB1/non-CB2 cannabinoid-like receptor, for example: an eating disorder; obesity; cardiovascular disease; a disease or disorder characterised by an addiction component; addiction; withdrawal; smoking addiction; smoking withdrawal; drug addiction; drug withdrawal; smoking cessation therapy; a bone disease or disorder; osteoporosis, Paget' s disease of bone; bone related cancer; breast cancer; breast cancer metastases; breast cancer which has metastasised to bone; cancer associated with activation or inactivation of a non-CB1/non-CB2 cannabinoid-like receptor,

摘要翻译： 本发明涉及大麻素（CB）受体和大麻素样受体中性拮抗剂，特别是式（I）的CB1中性拮抗剂。 本发明还涉及这些用于治疗通过用大麻素1型（CB1）受体或非CB1 /非CB2大麻素样受体的中性拮抗剂治疗而改善的疾病和病症的化合物，用于 例如：饮食失调; 肥胖; 心血管疾病; 以成瘾成分为特征的疾病或病症; 瘾; 退出; 吸烟成瘾; 戒烟 药物成瘾; 戒毒 戒烟治疗 骨病或病症; 骨质疏松症，佩吉特氏骨病; 骨相关癌症; 乳腺癌; 乳腺癌转移; 已经转移到骨骼的乳腺癌; 与非CB1 /非CB2大麻素样受体的活化或失活相关的癌症，