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1.发明授权Compounds with matrix-metalloproteinase inhibitory activity and imaging agents thereof 有权具有基质金属蛋白酶抑制活性的化合物及其成像剂公开(公告)号：US09023318B2
公开(公告)日：2015-05-05
申请号：US13849646
申请日：2013-03-25
申请人： Gang Chen , Umesh B. Gangadharmath , Dhanalakshmi Kasi , Harmuth C. Kolb , Changhui Liu , Anjana Sinha , Anna Katrin Szardenings , Joseph C. Walsh , Eric Wang , Chul Yu , Wei Zhang , Klaus Kopka , Guenter Haufe , Michael Schaefers , Verena Hugenberg , Stefan Wagner , Sven Hermann , Hans-Joerg Breyholz , Andreas Faust
发明人： Gang Chen , Umesh B. Gangadharmath , Dhanalakshmi Kasi , Harmuth C. Kolb , Changhui Liu , Anjana Sinha , Anna Katrin Szardenings , Joseph C. Walsh , Eric Wang , Chul Yu , Wei Zhang , Klaus Kopka , Guenter Haufe , Michael Schaefers , Verena Hugenberg , Stefan Wagner , Sven Hermann , Hans-Joerg Breyholz , Andreas Faust
IPC分类号： A61K51/00 , A61M36/14 , C07D403/14 , C07D405/14 , C07D249/04 , C07D309/12 , C07D213/42
CPC分类号： C07D403/14 , C07D213/42 , C07D249/04 , C07D309/12 , C07D405/14
摘要： Novel compounds and pharmaceutical compositions having MMP inhibitory activity are disclosed, which have been found to be particularly useful in the prevention, treatment and diagnostic imaging of diseases associated with an unpaired activity of MMP, amongst others MMP-2, MMP-8, MMP-9 and/or MMP-13 to name a few. The compounds of the present invention are useful for the prevention, the treatment and the in vivo diagnostic imaging of a range of disease states (inflammatory, malignant and degenerative diseases) where specific matrix metalloproteinases are known to be involved.
摘要翻译： 已经公开了具有MMP抑制活性的新型化合物和药物组合物，其已经被发现特别可用于预防，治疗和诊断成像与MMP的非配对活性相关的疾病，其中MMP-2，MMP-8，MMP- 9和/或MMP-13等等。 本发明的化合物可用于预防，治疗和体内诊断成像的一系列疾病状态（炎性，恶性和退行性疾病），其中已知特定的基质金属蛋白酶涉及。
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2.发明申请Compounds With Matrix-Metalloproteinase Inhibitory Activity and Imaging Agents Thereof 有权具有基质金属蛋白酶抑制活性和成像剂的化合物公开(公告)号：US20130217887A1
公开(公告)日：2013-08-22
申请号：US13849646
申请日：2013-03-25
申请人： Gang Chen , Umesh B. Gangadharmath , Dhanalakshmi Kasi , Harmuth C. Kolb , Changhui Liu , Anjana Sinha , Anna Katrin Szardenings , Joseph C. Walsh , Eric Wang , Chul Yu , Wei Zhang , Klaus Kopka , Guenter Haufe , Michael Schaefers , Verena Hugenberg , Stefan Wagner , Sven Hermann , Hans-Joerg Breyholz , Andreas Faust
发明人： Gang Chen , Umesh B. Gangadharmath , Dhanalakshmi Kasi , Harmuth C. Kolb , Changhui Liu , Anjana Sinha , Anna Katrin Szardenings , Joseph C. Walsh , Eric Wang , Chul Yu , Wei Zhang , Klaus Kopka , Guenter Haufe , Michael Schaefers , Verena Hugenberg , Stefan Wagner , Sven Hermann , Hans-Joerg Breyholz , Andreas Faust
IPC分类号： C07D403/14 , C07D249/04 , C07D405/14
CPC分类号： C07D403/14 , C07D213/42 , C07D249/04 , C07D309/12 , C07D405/14
摘要： Novel compounds and pharmaceutical compositions having MMP inhibitory activity are disclosed, which have been found to be particularly useful in the prevention, treatment and diagnostic imaging of diseases associated with an unpaired activity of MMP, amongst others MMP-2, MMP-8, MMP-9 and/or MMP-13 to name a few. The compounds of the present invention are useful for the prevention, the treatment and the in vivo diagnostic imaging of a range of disease states (inflammatory, malignant and degenerative diseases) where specific matrix metalloproteinases are known to be involved.
摘要翻译： 已经公开了具有MMP抑制活性的新型化合物和药物组合物，其已经被发现特别可用于预防，治疗和诊断成像与MMP的非配对活性相关的疾病，其中MMP-2，MMP-8，MMP- 9和/或MMP-13等等。 本发明的化合物可用于预防，治疗和体内诊断成像的一系列疾病状态（炎性，恶性和退行性疾病），其中已知特定的基质金属蛋白酶涉及。
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3.发明申请Compounds with Matrix-Metalloproteinase Inhibitory Activity and Imaging Agents Thereof 审中-公开具有基质金属蛋白酶抑制活性和成像剂的化合物公开(公告)号：US20120282180A1
公开(公告)日：2012-11-08
申请号：US13155558
申请日：2011-06-08
申请人： Hartmuth C. Kolb , Guenter Haufe , Malte Behrends , Klaus Kopka , Stefan Wagner , Verena Hugenberg , Hans-Joerg Breyholz , Sven Hermann , Michael Schaefers
发明人： Hartmuth C. Kolb , Guenter Haufe , Malte Behrends , Klaus Kopka , Stefan Wagner , Verena Hugenberg , Hans-Joerg Breyholz , Sven Hermann , Michael Schaefers
IPC分类号： A61K51/04 , A61K31/216 , C07D213/55 , A61K31/44 , A61P35/00 , A61K31/18 , C07D309/10 , A61K31/351 , A61P9/00 , A61P29/00 , C07C311/16 , A61K31/195
CPC分类号： C07C311/29 , C07D213/42 , C07D309/12
摘要： The present invention relates to the field of therapeutic and diagnostic agents and more specifically to compounds of formula (I) that are inhibitors of matrix-metalloproteinases (MMPs) and are useful in the treatment of diseases related thereto such as cardiovascular diseases, inflammatory diseases and malignant diseases. One embodiment of the invention is a compound of formula (I) labeled with a 18-fluorine atom having matrix metalloproteinase inhibitory activity suitable for diagnostic imaging. Also disclosed in the present invention is a pharmaceutical composition comprising the inhibitors of matrix-metalloproteinases (MMPs) of the invention or the corresponding labeled compounds useful as diagnostic imaging agents of the invention in a form suitable for mammalian administration. The invention furthermore discloses intermediates in the synthesis of the inhibitors of matrix-metalloproteinases (MMPs) of the invention and of the diagnostic imaging agents of the invention and kits for the preparation of the pharmaceutical composition of the invention.
摘要翻译： 本发明涉及治疗和诊断剂领域，更具体地涉及作为基质金属蛋白酶抑制剂（MMP）的式（I）化合物，可用于治疗与其相关的疾病如心血管疾病，炎性疾病和 恶性疾病。 本发明的一个实施方案是用具有适合于诊断成像的基质金属蛋白酶抑制活性的18-氟原子标记的式（I）化合物。 本发明还公开了一种药物组合物，其包含本发明的基质金属蛋白酶抑制剂（MMPs）或适用于哺乳动物给药形式的本发明诊断显像剂的相应标记化合物。 本发明还公开了合成本发明的基质金属蛋白酶抑制剂（MMPs）和本发明的诊断显像剂以及用于制备本发明的药物组合物的试剂盒的中间体。
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4.发明申请NEW LIGANDS FOR TARGETING OF S1P RECEPTORS FOR IN VIVO IMAGING AND TREATMENT OF DISEASES 有权用于影像检测和治疗疾病的S1P受体的新配体公开(公告)号：US20140170067A1
公开(公告)日：2014-06-19
申请号：US14237572
申请日：2012-08-16
IPC分类号： A61K51/04 , C07C311/41 , C07D401/14 , C07C215/10
CPC分类号： A61K51/04 , C07C215/10 , C07C233/18 , C07C311/41 , C07D401/14
摘要： The present invention relates to novel compounds of formulae (I) and (II) which are useful in the prevention, treatment and diagnosis, in vivo diagnosis of diseases or disorders related to S1P receptors, in particular, in diseases which are connected to the regulatory function of sphingosine-1-phosphate (S1P) and its analogues, such as inflammation, pain, autoimmune diseases and cardiovascular diseases.
摘要翻译： 本发明涉及新的式（I）和（II）化合物，其可用于预防，治疗和诊断与S1P受体相关的疾病或病症的体内诊断，特别是与调节相关的疾病 鞘氨醇-1-磷酸（S1P）及其类似物如炎症，疼痛，自身免疫性疾病和心血管疾病的功能。
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5.发明授权Ligands for targeting of S1P receptors for in vivo imaging and treatment of diseases 有权用于靶向S1P受体的配体用于体内成像和治疗疾病公开(公告)号：US09345791B2
公开(公告)日：2016-05-24
申请号：US14237572
申请日：2012-08-16
IPC分类号： A61K51/04 , C07C311/41 , C07C215/10 , C07C233/18 , C07D401/14
CPC分类号： A61K51/04 , C07C215/10 , C07C233/18 , C07C311/41 , C07D401/14
摘要： The present invention relates to novel compounds of formulae (I) and (II) which are useful in the prevention, treatment and diagnosis, in vivo diagnosis of diseases or disorders related to S1P receptors, in particular, in diseases which are connected to the regulatory function of sphingosine-1-phosphate (S1P) and its analogs, such as inflammation, pain, autoimmune diseases and cardiovascular diseases.
摘要翻译： 本发明涉及新的式（I）和（II）化合物，其可用于预防，治疗和诊断与S1P受体相关的疾病或病症的体内诊断，特别是与调节相关的疾病 鞘氨醇-1-磷酸（S1P）及其类似物的功能，如炎症，疼痛，自身免疫疾病和心血管疾病。
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