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1. 发明授权

US07745424B2 Alkane diol derivatives as therapeutic agents for the treatment of bone conditions 有权
标题翻译：烷基二醇衍生物作为治疗骨质的治疗剂
公开(公告)号：US07745424B2
公开(公告)日：2010-06-29
申请号：US10494327
申请日：2002-10-31
申请人： Stuart H Ralston , Iain R Greig , Robert J Van't Hof , Kenneth J Armour
发明人： Stuart H Ralston , Iain R Greig , Robert J Van't Hof , Kenneth J Armour
IPC分类号： A61K31/66 , A61K31/225
CPC分类号： A61K31/235
摘要： The present invention pertains to certain alkane diol derivatives (including, e.g., mono- and di-esters) of the formula R1—O-A-O—R2, wherein: A is a C2-10 alkylene group; R1 is independently a first hydroxy protecting group (e.g., an ester group); and, R2 is independently —H or a second hydroxy protecting group (e.g., an ester group); and pharmaceutically acceptable salts, solvates, amides, esters, ethers, chemically protected forms, and prodrug thereof, which, inter alia, inhibit osteoclast survival, formation, and/or activity; and/or inhibit bone resorption. 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, such as osteoporosis, rheumatoid arthritis, cancer associated bone disease, Paget's disease, and the like; and/or conditions associated with inflammation or activation of the immune system.
摘要翻译：本发明涉及式R 1 -O-A-O-R 2的某些烷二醇衍生物（包括例如单酯和二酯），其中：A是C 2-10亚烷基; R1独立地是第一羟基保护基（例如酯基）; 和R2独立地为-H或第二羟基保护基（例如酯基）; 其药学上可接受的盐，溶剂合物，酰胺，酯，醚，化学保护形式和前药，其尤其抑制破骨细胞存活，形成和/或活性; 和/或抑制骨吸收。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，例如骨质疏松症，类风湿性关节炎，癌症相关的骨病，佩吉特氏病等; 和/或与免疫系统的炎症或活化相关的病症。

2. 发明授权

US07598289B2 Ketones and reduced ketones as therapeutic agents for the treatment of bone conditions 有权
标题翻译：酮和还原酮作为治疗骨质素的治疗剂
公开(公告)号：US07598289B2
公开(公告)日：2009-10-06
申请号：US12193855
申请日：2008-08-19
申请人： Stuart H. Ralston , Iain R. Greig , Aymen I. I. Mohamed , Robert J. Van 'T Hof
发明人： Stuart H. Ralston , Iain R. Greig , Aymen I. I. Mohamed , Robert J. Van 'T Hof
IPC分类号： A61K31/185 , A61K31/22 , A61K31/15 , A61K31/12 , C07C49/00 , C07C207/00
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 and pharmaceutically acceptable salts, amides, esters, and ethers thereof, wherein: Ar1, Ralk, —ORO, and -Q are as defined herein: The present invention also pertains to pharmaceutical compositions comprising such compounds. The compounds inhibit osteoclast survival, formation, and/or activity, and inhibit conditions mediated by osteoclasts and/or characterised by bone resorption, and are useful 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; 酰胺，酯和醚类化合物，其中：Ar1，Ralk，-ORO和-Q如本文所定义：本发明还涉及涉及包含这些化合物的药物组合物。这些化合物抑制破骨细胞存活，形成和/或活性，并抑制破骨细胞介导的和/或由骨吸收特征，并且可用于治疗骨疾病如骨质疏松症，类风湿性关节炎，癌症相关的骨病，佩吉特氏病，假体植入物的无菌松动等; 和/或治疗与炎症或免疫系统的激活相关的病症。

3. 发明授权

US07572825B2 Ketones and reduced ketones as therapeutic agents for the treatment of bone conditions 有权
公开(公告)号：US07572825B2
公开(公告)日：2009-08-11
申请号：US10555738
申请日：2004-05-06
申请人： Stuart H. Ralston , Iain R. Greig , Aymen I. I. Mohamed , Robert J. Van 'T Hof
发明人： Stuart H. Ralston , Iain R. Greig , Aymen I. I. Mohamed , Robert J. Van 'T Hof
IPC分类号： A61K31/385 , A61K31/22 , A61K31/15 , 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: Ar1 is independently a biphenyl, phenanthryl, fluorenyl, or carbazolyl, and is optionally substituted; Ralk is independently a C2-10alkylene group, and is optionally substituted; —ORO, if present, is independently —OH or —ORK; —ORK, if present, is independently selected from: —O—RK1; —O—C(═O)RK2; —O—C(═O)ORK3; —O—S(═O)2ORK4; Q is independently —OH or —OROT; wherein: —OROT, if present, is independently selected from: —O—RE1; —O—C(═O)—RE2; —O—C(═O)—O—RE3; —O—C(═O)—O—SO3RE4; —O—C(═O)—O—(CH2)n—COORE5; —O—C(═O)—(CH2)n—NRN1RN2; —O—C(═O)—(CH2)n—NH—C(═O)RE6; —O—C(═O)—(CH2)n—C(═O)—NRN3RN4; —O—P(═O)(ORE7)(ORE8); —O—RPA; RPA, if present, is an organic group which incorporates a phosphonic acid group; with the proviso that if —OROT is —O—RE1, then RE1 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.

4. 发明申请

US20080312186A1 KETONES AND REDUCED KETONES AS THERAPEUTIC AGENTS FOR THE TREATMENT OF BONE CONDITIONS 有权
标题翻译：作为治疗骨质素的治疗药物的酮类和降低的克松顿
公开(公告)号：US20080312186A1
公开(公告)日：2008-12-18
申请号：US12193855
申请日：2008-08-19
申请人： Stuart H. RALSTON , Iain R. GREIG , Aymen I. I. MOHAMED , Robert J. VAN 'T HOF
发明人： Stuart H. RALSTON , Iain R. GREIG , Aymen I. I. MOHAMED , Robert J. VAN 'T HOF
IPC分类号： A61K31/695 , C07F7/02 , C07F7/08 , C07D339/08 , A61K31/385 , C07C49/303 , A61K31/12 , C07C63/00 , A61K31/19 , C07C233/00 , A61K31/164 , C07D309/02 , A61K31/35 , C07C33/00 , A61K31/045 , C07C43/02 , A61K31/075 , A61P19/08
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 and pharmaceutically acceptable salts, amides, esters, and ethers thereof, wherein: Ar1, Ralk, —ORO, and -Q are as defined herein: The present invention also pertains to pharmaceutical compositions comprising such compounds. The compounds inhibit osteoclast survival, formation, and/or activity, and inhibit conditions mediated by osteoclasts and/or characterised by bone resorption, and are useful 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; 酰胺，酯和醚类化合物，其中：Ar1，Ralk，-ORO和-Q如本文所定义：本发明还涉及涉及包含这些化合物的药物组合物。这些化合物抑制破骨细胞存活，形成和/或活性，并抑制破骨细胞介导的和/或由骨吸收特征，并且可用于治疗骨疾病如骨质疏松症，类风湿性关节炎，癌症相关的骨病，佩吉特氏病，假体植入物的无菌松动等; 和/或治疗与炎症或免疫系统的激活相关的病症。

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