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1.发明授权Val-pro containing .alpha.-keto oxadiazoles as serine protease inhibitors 失效含有α-酮恶二唑作为丝氨酸蛋白酶抑制剂的Val-pro
公开(公告)号：US6001813A
公开(公告)日：1999-12-14
申请号：US090046
申请日：1998-06-03
申请人： Albert C. Gyorkos , Lyle W. Spruce
发明人： Albert C. Gyorkos , Lyle W. Spruce
IPC分类号： A61K38/00 , C07D271/10 , C07D413/12 , C07D413/14 , C07D417/12 , C07K5/02 , C07K5/06 , C07K5/062 , C07K5/065 , C07K5/068 , C07K5/072 , C07K5/078 , C07K5/083 , C07K5/12 , A61K38/06
CPC分类号： C07D271/10 , C07D413/12 , C07D413/14 , C07D417/12 , C07K5/0202 , C07K5/06026 , C07K5/06043 , C07K5/06052 , C07K5/06078 , C07K5/06086 , C07K5/06104 , C07K5/06139 , C07K5/06156 , C07K5/06191 , C07K5/0806 , C07K5/12 , A61K38/00
摘要： The present invention relates to certain substituted oxadiazole tripeptides, which are useful as inhibitors of human neutrophil elastase (HNE) for the treatment of HNE-mediated processes implicated in conditions such as adult respiratory distress syndrome, septic shock and multiple organ failure. A series of studies also have indicated the involvement HNE in myocardial ischemia-reperfusion injury, emphysema. HNE-mediated processes are implicated in other conditions such as arthritis, periodontal disease, glomerulonephritis, dermatitis, psoriasis, cystic fibrosis, chronic bronchitis, atherosclerosis, Alzheimer's disease, organ transplantation, corneal ulcers, and invasion behavior of malignant tumors.
摘要翻译： 本发明涉及某些取代的恶二唑三肽，其可用作人嗜中性粒细胞弹性蛋白酶（HNE）的抑制剂，用于治疗涉及诸如成人呼吸窘迫综合征，败血性休克和多器官功能衰竭等病症的HNE介导的过程。 一系列研究也表明HNE参与心肌缺血再灌注损伤，肺气肿。 HNE介导的过程涉及诸如关节炎，牙周病，肾小球性肾炎，皮炎，牛皮癣，囊性纤维化，慢性支气管炎，动脉粥样硬化，阿尔茨海默氏病，器官移植，角膜溃疡和恶性肿瘤的侵袭行为等其他病症。
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2.发明授权Indole and tetrahydroisoquinoline containing Alpha-keto oxadiazoles as serine protease inhibitors 失效含有α-酮基恶二唑的吲哚和四氢异喹啉作为丝氨酸蛋白酶抑制剂
公开(公告)号：US6100238A
公开(公告)日：2000-08-08
申请号：US89587
申请日：1998-06-03
申请人： Albert C. Gyorkos , Lyle W. Spruce
发明人： Albert C. Gyorkos , Lyle W. Spruce
IPC分类号： A61K38/00 , C07D271/10 , C07D413/12 , C07D413/14 , C07D417/12 , C07K5/02 , C07K5/06 , C07K5/062 , C07K5/065 , C07K5/068 , C07K5/072 , C07K5/078 , C07K5/083 , C07K5/12 , A61K38/05 , A61K38/06
CPC分类号： C07D271/10 , C07D413/12 , C07D413/14 , C07D417/12 , C07K5/06052 , C07K5/06139 , C07K5/06165 , A61K38/00
摘要： The present invention relates to certain substituted oxadiazole nonpeptides, which are useful as inhibitors of human neutrophil elastase (HNE) for the treatment of HNE-mediated processes implicated in conditions such as adult respiratory distress syndrome, septic shock and multiple organ failure. A series of studies also have indicated the involvement HNE in myocardial ischemia-reperfusion injury, emphysema. HNE-mediated processes are implicated in other conditions such as arthritis, periodontal disease, glomerulonephritis, dermatitis, psoriasis, cystic fibrosis, chronic bronchitis, atherosclerosis, Alzheimer's disease, organ transplantation, corneal ulcers, and invasion behavior of malignant tumors.
摘要翻译： 本发明涉及某些取代的恶二唑非肽，其可用作人嗜中性粒细胞弹性蛋白酶（HNE）的抑制剂，用于治疗涉及诸如成人呼吸窘迫综合征，败血性休克和多器官功能衰竭等病症的HNE介导的过程。 一系列研究也表明HNE参与心肌缺血再灌注损伤，肺气肿。 HNE介导的过程涉及诸如关节炎，牙周病，肾小球性肾炎，皮炎，牛皮癣，囊性纤维化，慢性支气管炎，动脉粥样硬化，阿尔茨海默氏病，器官移植，角膜溃疡和恶性肿瘤的侵袭行为等其他病症。
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公开(公告)号：US6159938A
公开(公告)日：2000-12-12
申请号：US859242
申请日：1997-05-20
IPC分类号： A61K38/00 , C07D271/10 , C07D413/12 , C07D413/14 , C07D417/12 , C07K5/02 , C07K5/06 , C07K5/062 , C07K5/065 , C07K5/068 , C07K5/072 , C07K5/078 , C07K5/083 , C07K5/12 , A61K38/05 , A61K38/06 , A61K38/07 , A61K38/08
CPC分类号： C07D271/10 , A61K38/00 , C07D413/12 , C07D413/14 , C07D417/12 , C07K5/0202 , C07K5/06026 , C07K5/06043 , C07K5/06052 , C07K5/06165 , C07K5/06191 , C07K5/0806 , C07K5/0808 , C07K5/0821 , C07K5/12 , Y02A50/423
摘要： Provided are methods of inhibiting the activity of a serine protease using protease inhibitors that include an alpha-keto heterocycle in their structure. The methods are useful in the treatment of ischemic heart or treatment of symptoms associated with blood coagulation disorders. Also provided are methods for detecting or quantifying the activity of a serine protease in a pure sample.
摘要翻译： 提供的是使用蛋白酶抑制剂来抑制丝氨酸蛋白酶的活性的方法，所述蛋白酶抑制剂在其结构中包括α-酮杂环。 该方法可用于治疗缺血性心脏或治疗与凝血障碍相关的症状。 还提供了用于检测或定量纯样品中丝氨酸蛋白酶的活性的方法。
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公开(公告)号：US6150334A
公开(公告)日：2000-11-21
申请号：US985201
申请日：1997-12-04
申请人： Albert C. Gyorkos , Lyle W. Spruce
发明人： Albert C. Gyorkos , Lyle W. Spruce
IPC分类号： A61K38/00 , C07D271/10 , C07D413/12 , C07D413/14 , C07D417/12 , C07K5/02 , C07K5/06 , C07K5/062 , C07K5/065 , C07K5/068 , C07K5/072 , C07K5/078 , C07K5/083 , C07K5/12 , A61K38/06
CPC分类号： C07D271/10 , C07D413/12 , C07D413/14 , C07D417/12 , C07K5/0202 , C07K5/06026 , C07K5/06052 , C07K5/06139 , C07K5/06191 , C07K5/0806 , C07K5/0808 , C07K5/0821 , C07K5/0827 , C07K5/12 , A61K38/00
摘要： The present invention relates to certain compounds comprising substituted oxadiazole, thiadiazole and triazole structures which are useful as inhibitors of serine proteases, including human neutrophil elastase (HNE). Compounds described herein are characterized by their relatively low molecular weight, high potency and selectivity with respect to HNE, and can be used to effectively prevent, alleviate or otherwise treat disease states characterized by the degradation of connective tissue by proteases in humans.
摘要翻译： 本发明涉及可用作丝氨酸蛋白酶抑制剂（包括人嗜中性粒细胞弹性蛋白酶（HNE））的取代恶二唑，噻二唑和三唑结构的某些化合物。 本文描述的化合物的特征在于其相对于HNE相对低的分子量，高效力和选择性，并且可用于有效地预防，减轻或以其他方式治疗以人类中蛋白酶降解结缔组织为特征的疾病状态。
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公开(公告)号：US6004933A
公开(公告)日：1999-12-21
申请号：US065258
申请日：1998-04-23
申请人： Lyle W. Spruce , Albert C. Gyorkos , John C. Cheronis , Val S. Goodfellow , Axel H. Leimer , John M. Young , James Ivan Gerrity
发明人： Lyle W. Spruce , Albert C. Gyorkos , John C. Cheronis , Val S. Goodfellow , Axel H. Leimer , John M. Young , James Ivan Gerrity
IPC分类号： A61K38/00 , C07K5/06 , C07K5/062 , C07K5/087 , C07K5/093 , A61K38/03 , C07D215/02 , C07D237/30 , C07D239/70 , C07D241/36 , C07D253/10
CPC分类号： C07K5/06078 , C07K5/06043 , C07K5/06052 , C07K5/0812 , C07K5/0819 , A61K38/00
摘要： The present invention relates to cysteine protease inhibitors of the general formula (I): ##STR1## wherein Z is a cysteine protease binding moiety; X and Y are S, O or optionally substituted N; and R.sub.1 is optionally substituted alkyl or aryl.
摘要翻译： 本发明涉及通式（I）的半胱氨酸蛋白酶抑制剂：其中Z是半胱氨酸蛋白酶结合部分; X和Y是S，O或任选取代的N; 并且R 1是任选取代的烷基或芳基。
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公开(公告)号：US6001814A
公开(公告)日：1999-12-14
申请号：US90274
申请日：1998-06-03
申请人： Albert C. Gyorkos , Lyle W. Spruce
发明人： Albert C. Gyorkos , Lyle W. Spruce
IPC分类号： A61K38/00 , C07D271/10 , C07D413/12 , C07D413/14 , C07D417/12 , C07K5/02 , C07K5/06 , C07K5/062 , C07K5/065 , C07K5/068 , C07K5/072 , C07K5/078 , C07K5/083 , C07K5/12 , A61K38/05 , A61K38/06
CPC分类号： C07D271/10 , C07D413/12 , C07D413/14 , C07D417/12 , C07K5/0202 , C07K5/06026 , C07K5/06043 , C07K5/06052 , C07K5/06078 , C07K5/06086 , C07K5/06104 , C07K5/06139 , C07K5/06156 , C07K5/06191 , C07K5/0806 , C07K5/12 , A61K38/00
摘要： The present invention relates to certain substituted oxadiazole nonpeptides, which are useful as inhibitors of human neutrophil elastase (HNE) for the treatment of HNE-mediated processes implicated in conditions such as adult respiratory distress syndrome, septic shock and multiple organ failure. A series of studies also have indicated the involvement HNE in myocardial ischemia-reperfusion injury, emphysema. HNE-mediated processes are implicated in other conditions such as arthritis, periodontal disease, glomerulonephritis, dermatitis, psoriasis, cystic fibrosis, chronic bronchitis, atherosclerosis, Alzheimer's disease, organ transplantation, corneal ulcers, and invasion behavior of malignant tumors.
摘要翻译： 本发明涉及某些取代的恶二唑非肽，其可用作人嗜中性粒细胞弹性蛋白酶（HNE）的抑制剂，用于治疗涉及诸如成人呼吸窘迫综合征，败血性休克和多器官功能衰竭等病症的HNE介导的过程。 一系列研究也表明HNE参与心肌缺血再灌注损伤，肺气肿。 HNE介导的过程涉及诸如关节炎，牙周病，肾小球性肾炎，皮炎，牛皮癣，囊性纤维化，慢性支气管炎，动脉粥样硬化，阿尔茨海默氏病，器官移植，角膜溃疡和恶性肿瘤的侵袭行为等其他病症。
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