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1.发明授权NAALADase inhibitors useful as pharmaceutical compounds and compositions 失效用作药物化合物和组合物的NAALADase抑制剂公开(公告)号：US06458775B1
公开(公告)日：2002-10-01
申请号：US09346711
申请日：1999-07-02
申请人： Paul F. Jackson , Keith M. Maclin , Eric Wang , Barbara S. Slusher , Rena S. Lapidus , Pavel Majer
发明人： Paul F. Jackson , Keith M. Maclin , Eric Wang , Barbara S. Slusher , Rena S. Lapidus , Pavel Majer
IPC分类号： A61K3166
CPC分类号： C07C309/17 , C07C309/24 , C07C317/44 , C07C323/12 , C07C323/52 , C07C323/56 , C07C327/18 , C07C327/36 , C07C329/12 , C07C333/14 , C07C333/20 , C07D213/55
摘要： The present invention relates to N-Acetylated &agr;-Linked Acidic Dipeptidase (NAALADase) inhibitors enzyme activity, pharmaceutical compositions comprising such inhibitors, and methods of their use to inhibit NAALADase enzyme activity, thereby effecting neuronal activities, inhibiting angiogenesis, and treating glutamate abnormalities, compulsive disorders, prostate diseases, pain and diabetic neuropathy.
摘要翻译： 本发明涉及N-乙酰化的α-连接酸性二肽酶（NAALADase）抑制剂酶活性，包含这些抑制剂的药物组合物及其用于抑制NAALADase酶活性的方法，从而影响神经元活性，抑制血管发生和治疗谷氨酸异常， 强迫症，前列腺疾病，疼痛和糖尿病性神经病变。
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公开(公告)号：US06265609B1
公开(公告)日：2001-07-24
申请号：US09228391
申请日：1999-01-12
IPC分类号： C07C5502
CPC分类号： C07C323/56 , C07C323/52
摘要： The present invention relate to thio-substituted pentanedioic acid derivatives that inhibit N-Acetylated &agr;-Linked Acidic Dipeptidase (NAALADase) enzyme activity, pharmaceutical compositions comprising the same, and methods of using the same to inhibit NAALADase enzyme activity, to effect neuronal activities, to inhibit angiogenesis, and to treat glutamate abnormalities, compulsive disorders and prostate diseases.
摘要翻译： 本发明涉及抑制N-乙酰化α链接酸性二肽酶（NAALADase）酶活性的硫代取代戊二酸衍生物，包含其的药物组合物及其用于抑制NAALADase酶活性，影响神经元活性的方法， 抑制血管发生，并治疗谷氨酸异常，强迫症和前列腺疾病。
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公开(公告)号：US6054444A
公开(公告)日：2000-04-25
申请号：US842360
申请日：1997-04-24
IPC分类号： A61K31/194 , A61K38/05 , A61K38/06 , A61P21/00 , C07F9/30 , A61K31/675 , A61K31/66 , A61K31/665 , A61K31/67 , C07F9/40 , C07F9/572 , C07F9/58 , C07F9/655 , C07F9/6553
CPC分类号： A61K31/661 , A61K31/194 , A61K38/05 , A61K38/06 , C07F9/301
摘要： The present invention relates to phosphonic acid derivatives that inhibit N-Acetylated .alpha.-Linked Acidic Dipeptidase (NAALADase) enzyme activity, pharmaceutical compositions comprising such derivatives, and methods of using such derivatives to inhibit NAALADase activity, to treat a glutamate abnormality and to treat a prostate disease in an animal.
摘要翻译： 本发明涉及抑制N-乙酰化的α-脱羧酸性二肽酶（NAALADase）酶活性的膦酸衍生物，包含这些衍生物的药物组合物，以及使用这些衍生物抑制NAALADase活性的方法，治疗谷氨酸异常和治疗 动物前列腺疾病。
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公开(公告)号：US6046180A
公开(公告)日：2000-04-04
申请号：US863624
申请日：1997-05-27
IPC分类号： A61K31/662 , A61K31/194 , A61K31/665 , A61K31/67 , A61K31/675 , A61K38/05 , A61K38/06 , A61P13/08 , A61P35/00 , A61P43/00 , C07F9/30 , C07F9/38 , C07F9/40 , C07F9/44 , C07F9/58 , C07F9/655 , C07F9/6553 , A61K31/685 , C07F9/22
CPC分类号： A61K31/661 , A61K31/194 , A61K38/05 , A61K38/06 , C07F9/301 , C07F9/3808 , C07F9/3826 , C07F9/4075 , C07F9/4465 , C07F9/582 , C07F9/65515 , C07F9/6552 , C07F9/655345
摘要： The present disclosure relates to dipeptidase inhibitors, and more particularly, to novel phosphonate derivatives, hydroxyphosphinyl derivatives, and phosphoramidate derivatives that inhibit N-Acetylated .alpha.-Linked Acidic Dipeptidase (NAALADase) enzyme activity, pharmaceutical compositions comprising such derivatives, and methods of using such derivatives to inhibit NAALADase activity, and to treat prostate diseases, especially using the compounds of the present invention for the inhibition of the growth of prostate cancer cells.
摘要翻译： 本公开内容涉及二肽酶抑制剂，更具体地涉及抑制N-乙酰化α-脱氢酸二肽酶（NAALADase）酶活性的新型膦酸酯衍生物，羟基氧膦基衍生物和氨基磷酸酯衍生物，包含该衍生物的药物组合物及其使用方法 抑制NAALADase活性的衍生物，以及治疗前列腺疾病，特别是使用本发明化合物抑制前列腺癌细胞的生长。
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公开(公告)号：US5902817A
公开(公告)日：1999-05-11
申请号：US835572
申请日：1997-04-09
IPC分类号： C07D213/71 , A61K31/194 , A61K31/4409 , A61K38/05 , A61K38/06 , A61P13/08 , A61P35/00 , C07C317/44 , C07C381/10 , C07F9/30 , A61K31/44 , A61K31/19 , C07C317/06
CPC分类号： A61K31/661 , A61K31/194 , A61K38/05 , A61K38/06 , C07F9/301
摘要： The present invention relates to thio derivatives that inhibit N-Acetylated .alpha.-Linked Acidic Dipeptidase (NAALADase) enzyme activity, pharmaceutical compositions comprising such derivatives, and methods of using such derivatives to inhibit NAALADase activity, to treat a glutamate abnormality and to treat a prostate disease in an animal.
摘要翻译： 本发明涉及抑制N-乙酰化的α-脱羧酸性二肽酶（NAALADase）酶活性的硫代衍生物，包含这些衍生物的药物组合物，以及使用这些衍生物抑制NAALADase活性的方法，治疗谷氨酸异常和治疗前列腺 动物疾病
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公开(公告)号：US5863536A
公开(公告)日：1999-01-26
申请号：US778733
申请日：1996-12-31
IPC分类号： A61K31/194 , A61K38/05 , A61K38/06 , C07F9/30 , C07F9/40 , C07F9/44 , C07F9/58 , C07F9/655 , A61K39/395
CPC分类号： A61K31/661 , A61K31/194 , A61K38/05 , A61K38/06 , C07F9/301 , C07F9/4075 , C07F9/4465 , C07F9/582 , C07F9/65515 , C07F9/6552
摘要： The present invention includes phosphoramidate derivatives, compositions containing the same, and methods of using them as NAALADase inhibitors, particularly for the treatment of glutamate abnormalities and associated nervous tissue insult in a animal and for treatment of prostate disease and prostate cancer by inhibition of NAALADase enzyme.
摘要翻译： 本发明包括氨基磷酸酯衍生物，含有它们的组合物以及使用它们作为NAALADase抑制剂的方法，特别是用于治疗动物中的谷氨酸异常和相关的神经组织损伤以及通过抑制NAALADase酶来治疗前列腺疾病和前列腺癌 。
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公开(公告)号：US5795877A
公开(公告)日：1998-08-18
申请号：US775586
申请日：1996-12-31
IPC分类号： A61K31/194 , A61K38/05 , A61K38/06 , C07F9/30 , C07F9/40 , C07F9/44 , C07F9/58 , C07F9/655 , C07F9/38 , A61K31/66
CPC分类号： A61K31/661 , A61K31/194 , A61K38/05 , A61K38/06 , C07F9/301 , C07F9/4075 , C07F9/4465 , C07F9/582 , C07F9/65515 , C07F9/6552
摘要： The present invention includes compounds, compositions, and methods of treatment for glutamate abnormalities and associated nervous tissue insult in a animal by inhibition of NAALADase enzyme. Compositions include phosphonate derivatives and mixtures thereof that inhibit NAALADase enzyme activity and their use for treating glutamate abnormalities such as created by global and focal ischemia and for treatment of prostate disease and prostate cancer by inhibition of NAALADase enzyme.
摘要翻译： 本发明包括通过抑制NAALADase酶在动物中治疗谷氨酸异常和相关神经组织损伤的化合物，组合物和方法。 组合物包括抑制NAALADase酶活性的膦酸酯衍生物及其混合物，以及它们用于治疗由全球和局部缺血引起的谷氨酸异常以及通过抑制NAALADase酶治疗前列腺疾病和前列腺癌的用途。
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8.发明授权Pharmaceutical compositions and methods of effecting a neuronal activity in an animal using naaladase inhibitors 失效使用奈拉替酶抑制剂在动物中进行神经元活性的药物组合物和方法公开(公告)号：US06413948B1
公开(公告)日：2002-07-02
申请号：US09388442
申请日：1999-09-02
IPC分类号： A61K3166
CPC分类号： A61K31/661 , A61K31/194 , A61K31/665 , A61K31/675 , A61K38/05 , A61K38/06 , C07F9/301 , C07F9/3808 , C07F9/3826 , C07F9/4075 , C07F9/4465 , C07F9/58 , C07F9/65515 , C07F9/6552 , C07F9/655345
摘要： The present invention relates to a method of treating a glutamate abnormality and a method of effecting a neuronal activity in an animal using a NAALADase inhibitor, and a pharmaceutical composition comprising an effective amount of a NAALADase inhibitor for treating a glutamate abnormality and effecting a neuronal activity in an animal.
摘要翻译： 本发明涉及一种治疗谷氨酸异常的方法和使用NAALADase抑制剂在动物中进行神经元活性的方法，以及包含有效量的用于治疗谷氨酸异常和影响神经元活性的NAALADase抑制剂的药物组合物 在一个动物
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公开(公告)号：US06372726B1
公开(公告)日：2002-04-16
申请号：US09405842
申请日：1999-09-27
IPC分类号： A61K3166
CPC分类号： A61K31/661 , A61K31/00 , A61K31/66 , A61K31/662 , A61K31/664 , A61K31/665 , A61K31/67 , A61K31/675 , C07F9/301 , C07F9/3808 , C07F9/3826 , Y10S514/908
摘要： The present disclosure relates to dipeptidase inhibitors, and more particularly, to novel methods of using phosphonate derivatives, hydroxyphosphinyl derivatives, and phosphoramidate derivatives to inhibit N-Acetylated &agr;-Linked Acidic Dipeptidase (NAALADase) enzyme activity, and to treat prostate diseases, especially using the compounds of the present invention for the inhibition of the growth of prostate cancer cells.
摘要翻译： 本公开内容涉及二肽酶抑制剂，更具体地涉及使用膦酸酯衍生物，羟基氧膦基衍生物和氨基磷酸酯衍生物抑制N-乙酰化α链接酸性二肽酶（NAALADase）酶活性并治疗前列腺疾病的新方法，特别是使用 用于抑制前列腺癌细胞生长的本发明化合物。
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公开(公告)号：US06271245B1
公开(公告)日：2001-08-07
申请号：US09322688
申请日：1999-06-01
IPC分类号： C07D21326
CPC分类号： A61K31/661 , A61K31/194 , A61K38/05 , A61K38/06 , C07F9/301
摘要： The present invention relates to hydroxamic acid derivatives that inhibit N-Acetylated &agr;-Linked Acidic Dipeptidase (NAALADase) enzyme activity, pharmaceutical compositions comprising such derivatives, and methods of using such derivatives to inhibit NAALADase activity, to treat a glutamate abnormality and to treat a prostate disease in an animal.
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