公开(公告)号：WO1997048409A1

公开(公告)日：1997-12-24

申请号：PCT/US1997010149

申请日：1997-06-13

Applicant: GUILFORD PHARMACEUTICALS INC.

Inventor： GUILFORD PHARMACEUTICALS INC. ,  SLUSHER, Barbara, S. ,  JACKSON, Paul, F. ,  TAYS, Kevin, L. ,  MACLIN, Keith, M.

IPC: A61K38/05

CPC classification number: A61K31/661 ,  A61K31/00 ,  A61K31/66 ,  A61K31/662 ,  A61K31/664 ,  A61K31/665 ,  A61K31/67 ,  A61K31/675 ,  C07F9/301 ,  C07F9/3808 ,  C07F9/3826

Abstract: 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 alpha -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.

Abstract translation: 本公开涉及二肽酶抑制剂，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-乙酰化的α-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。

公开(公告)号：WO1997048399A1

公开(公告)日：1997-12-24

申请号：PCT/US1997011538

申请日：1997-06-16

Applicant: GUILFORD PHARMACEUTICALS INC.

Inventor： GUILFORD PHARMACEUTICALS INC. ,  JACKSON, Paul, F. ,  SLUSHER, Barbara, S. ,  TAYS, Kevin, L. ,  MACLIN, Keith, M.

IPC: A61K31/66

CPC classification number: A61K31/661 ,  A61K31/194 ,  A61K38/05 ,  A61K38/06 ,  C07F9/301 ,  C07F9/3808 ,  C07F9/3826 ,  C07F9/4075 ,  C07F9/4465 ,  C07F9/58 ,  C07F9/65515 ,  C07F9/6552 ,  C07F9/655345

Abstract: 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.

Abstract translation: 本公开内容涉及二肽酶抑制剂，更具体地涉及新的膦酸酯衍生物，羟基氧膦基衍生物和抑制N-乙酰化的α-酸性二肽酶（NAALADase）酶活性的氨基磷酸酯衍生物，包含这些衍生物的药物组合物，以及使用这些衍生物的方法 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。

公开(公告)号：WO1998013046A1

公开(公告)日：1998-04-02

申请号：PCT/US1997014344

申请日：1997-08-15

Applicant: GUILFORD PHARMACEUTICALS INC.

Inventor： GUILFORD PHARMACEUTICALS INC. ,  SLUSHER, Barbara, S. ,  JACKSON, Paul, F. ,  TAYS, Kevin, L. ,  MACLIN, Keith, M.

IPC: A61K31/66

CPC classification number: 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

Abstract: 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.

Abstract translation: 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

公开(公告)号：WO1998013044A1

公开(公告)日：1998-04-02

申请号：PCT/US1997014417

申请日：1997-08-15

Applicant: GUILFORD PHARMACEUTICALS INC.

Inventor： GUILFORD PHARMACEUTICALS INC. ,  SLUSHER, Barbara, S. ,  JACKSON, Paul, F. ,  TAYS, Kevin, L. ,  MACLIN, Keith, M.

IPC: A61K31/44

CPC classification number: A61K31/661 ,  A61K31/194 ,  A61K31/665 ,  A61K31/675 ,  A61K38/05 ,  A61K38/06 ,  C07F9/301 ,  C07F9/3808 ,  C07F9/3826

Abstract: The present invention relates to a pharmaceutical composition and a method for treating a compulsive disorder using a NAALADase inhibitor.

Abstract translation: 本发明涉及药物组合物和使用NAALADase抑制剂治疗强迫症的方法。

公开(公告)号：WO1998053812A1

公开(公告)日：1998-12-03

申请号：PCT/US1997014347

申请日：1997-08-15

Applicant: GUILFORD PHARMACEUTICALS INC.

Inventor： GUILFORD PHARMACEUTICALS INC. ,  JACKSON, Paul, F. ,  SLUSHER, Barbara, S. ,  TAYS, Kevin, L. ,  MACLIN, Keith, M.

IPC: A61K31/34

CPC classification number: A61K31/661 ,  A61K31/194 ,  A61K38/05 ,  A61K38/06 ,  C07F9/301 ,  C07F9/3808 ,  C07F9/3826

Abstract: 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 alpha -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.

Abstract translation: 本公开涉及二肽酶抑制剂，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-乙酰化的α-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。

公开(公告)号：WO1997048400A1

公开(公告)日：1997-12-24

申请号：PCT/US1997011540

申请日：1997-06-16

Applicant: GUILFORD PHARMACEUTICALS INC.

Inventor： GUILFORD PHARMACEUTICALS INC. ,  JACKSON, Paul, F. ,  SLUSHER, Barbara, S. ,  TAYS, Kevin, L. ,  MACLIN, Keith, M.

IPC: A61K31/66

CPC classification number: A61K31/661 ,  A61K31/194 ,  A61K38/05 ,  A61K38/06 ,  C07F9/301 ,  C07F9/3808 ,  C07F9/3826 ,  C07F9/4075 ,  C07F9/4465 ,  C07F9/58 ,  C07F9/65515 ,  C07F9/6552 ,  C07F9/655345

Abstract: 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.

Abstract translation: 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。