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公开(公告)号：US5723459A
公开(公告)日：1998-03-03
申请号：US377315
申请日：1995-01-24
IPC分类号： C07D207/16 , C07D211/60 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/12 , C07D471/04 , C07D473/00 , A61K31/54 , A61K31/535 , C07D401/02 , C07D403/02
CPC分类号： C07D207/16 , C07D211/60 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/12 , C07D471/04 , C07D473/00
摘要： The present invention relates to novel compounds which possess a broad range of useful biological activities. These compounds can maintain, increase, or restore sensitivity of cells to therapeutic or prophylactic agents. They can also suppress, modify, or significantly reduce an immune response, including an autoimmune response in a mammal. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well-suited for treatment of multi-drug resistant cells, for prevention of the development of multi-drug resistance, for use in multi-drug resistant cancer therapy, and for prevention or treatment of graft rejection and various autoimmune diseases.
摘要翻译： 本发明涉及具有广泛有用生物活性的新化合物。 这些化合物可以维持，增加或恢复细胞对治疗或预防剂的敏感性。 它们还可以抑制，修饰或显着降低免疫应答，包括哺乳动物的自身免疫反应。 本发明还涉及包含这些化合物的药物组合物。 本发明的化合物和药物组合物特别适用于治疗多药耐药性细胞，用于预防多药耐药性的发展，用于多药耐药性癌症治疗以及用于预防或治疗移植物 排斥反应和各种自身免疫性疾病。
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公开(公告)号：US5620971A
公开(公告)日：1997-04-15
申请号：US217982
申请日：1994-03-25
IPC分类号： C07D207/16 , C07D211/60 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/12 , C07D471/04 , C07D473/00 , A61K31/54 , A61K31/535 , C07D403/06 , C07D403/14
CPC分类号： C07D401/12 , C07D207/16 , C07D211/60 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/12 , C07D471/04 , C07D473/00
摘要： The present invention relates to novel compounds which possess a broad range of useful biological activities. These compounds can maintain, increase, or restore sensitivity of cells to therapeutic or prophylactic agents. They can also suppress, modify, or significantly reduce an immune response, including an autoimmune response in a mammal. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well-suited for treatment of multi-drug resistant cells, for prevention of the development of multi-drug resistance, for use in multi-drug resistant cancer therapy, and for prevention or treatment of graft rejection and various autoimmune diseases.
摘要翻译： 本发明涉及具有广泛有用生物活性的新化合物。 这些化合物可以维持，增加或恢复细胞对治疗或预防剂的敏感性。 它们还可以抑制，修饰或显着降低免疫应答，包括哺乳动物的自身免疫反应。 本发明还涉及包含这些化合物的药物组合物。 本发明的化合物和药物组合物特别适用于治疗多药耐药性细胞，用于预防多药耐药性的发展，用于多药耐药性癌症治疗以及用于预防或治疗移植物 排斥反应和各种自身免疫性疾病。
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公开(公告)号：US5516797A
公开(公告)日：1996-05-14
申请号：US226011
申请日：1994-04-11
IPC分类号： A61K31/34 , A61K31/16 , A61K31/165 , A61K31/341 , A61K31/343 , A61K31/357 , A61K31/36 , A61K31/38 , A61K31/381 , A61K31/395 , A61K31/40 , A61K31/401 , A61K31/4025 , A61K31/4427 , A61K31/443 , A61K31/4439 , A61K31/445 , A61K31/4525 , A61K31/453 , A61K31/454 , A61K31/4545 , A61P25/02 , A61P37/06 , C07C233/56 , C07C235/12 , C07C235/34 , C07D207/08 , C07D207/16 , C07D211/60 , C07D307/54 , C07D317/60 , C07D333/24 , C07D401/06 , C07D401/12 , C07D403/06 , C07D405/06 , C07D409/06 , A61K31/22 , A61K31/24
CPC分类号： C07D401/06 , C07C233/56 , C07C235/34 , C07D211/60 , C07D317/60 , C07D403/06 , C07D405/06 , Y10S514/885
摘要： This invention relates to a novel class of immunosuppressive compounds having an affinity for the FK-506 binding protein (FKBP). Once bound to this protein, the immunosuppressive compounds inhibit the prolyl peptidyl cis-trans isomerase (rotamase) activity of the FKBP and inhibit T cell activation. As such, the compounds of this invention can be used as immunosuppressive drugs to prevent or significantly reduce graft rejection in bone marrow and organ transplantations and for use in the treatment of a wide variety of autoimmune diseases in humans and other mammals.
摘要翻译： 本发明涉及对FK-506结合蛋白（FKBP）具有亲和力的新一类免疫抑制化合物。 一旦结合到该蛋白质上，免疫抑制化合物抑制FKBP的脯氨酰基顺式 - 反式异构酶（旋转异构酶）活性并抑制T细胞活化。 因此，本发明的化合物可用作免疫抑制药物，以预防或显着降低骨髓和器官移植中的移植排斥反应，并用于治疗人类和其他哺乳动物中各种自身免疫性疾病。
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公开(公告)号：US5330993A
公开(公告)日：1994-07-19
申请号：US724734
申请日：1991-07-02
IPC分类号： A61K31/34 , A61K31/16 , A61K31/165 , A61K31/341 , A61K31/343 , A61K31/357 , A61K31/36 , A61K31/38 , A61K31/381 , A61K31/395 , A61K31/40 , A61K31/401 , A61K31/4025 , A61K31/4427 , A61K31/443 , A61K31/4439 , A61K31/445 , A61K31/4525 , A61K31/453 , A61K31/454 , A61K31/4545 , A61P25/02 , A61P37/06 , C07C233/56 , C07C235/12 , C07C235/34 , C07D207/08 , C07D207/16 , C07D211/60 , C07D307/54 , C07D317/60 , C07D333/24 , C07D401/06 , C07D401/12 , C07D403/06 , C07D405/06 , C07D409/06
CPC分类号： C07D401/06 , C07C233/56 , C07C235/34 , C07D211/60 , C07D317/60 , C07D403/06 , C07D405/06 , Y10S514/885
摘要： This invention relates to a novel class of immunosuppressive compounds having an affinity for the FK-506 binding protein (FKBP). Once bound to this protein, the immunosuppressive compounds inhibit the prolyl peptidyl cis-trans isomerase (rotamass) activity of the FKBP and inhibit T cell activation. As such, the compounds of this invention can be used as immunosuppressive drugs to prevent or significantly reduce graft rejection in bone marrow and organ transplantations and for use in the treatment of a wide variety of autoimmune diseases in humans and other mammals.
摘要翻译： 本发明涉及对FK-506结合蛋白（FKBP）具有亲和力的新一类免疫抑制化合物。 一旦结合到该蛋白质上，免疫抑制化合物抑制FKBP的脯氨酰基顺反异构酶（旋转异构体）活性并抑制T细胞活化。 因此，本发明的化合物可用作免疫抑制药物，以预防或显着降低骨髓和器官移植中的移植排斥反应，并用于治疗人类和其他哺乳动物中各种自身免疫性疾病。
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公开(公告)号：US5665774A
公开(公告)日：1997-09-09
申请号：US027870
申请日：1993-03-08
IPC分类号： A61K31/34 , A61K31/16 , A61K31/165 , A61K31/341 , A61K31/343 , A61K31/357 , A61K31/36 , A61K31/38 , A61K31/381 , A61K31/395 , A61K31/40 , A61K31/401 , A61K31/4025 , A61K31/4427 , A61K31/443 , A61K31/4439 , A61K31/445 , A61K31/4525 , A61K31/453 , A61K31/454 , A61K31/4545 , A61P25/02 , A61P37/06 , C07C233/56 , C07C235/12 , C07C235/34 , C07D207/08 , C07D207/16 , C07D211/60 , C07D307/54 , C07D317/60 , C07D333/24 , C07D401/06 , C07D401/12 , C07D403/06 , C07D405/06 , C07D409/06 , C07C229/36 , C07C229/24
CPC分类号： C07D401/06 , C07C233/56 , C07C235/34 , C07D211/60 , C07D317/60 , C07D403/06 , C07D405/06 , Y10S514/885
摘要： This invention relates to a novel class of immunosuppressive compounds having an affinity for the FK-506 binding protein (FKBP). Once bound to this protein, the immunosuppressive compounds inhibit the prolyl peptidyl cis-trans isomerase (rotamase) activity of the FKBP and inhibit T cell activation. As such, the compounds of this invention can be used as immunosuppressive drugs to prevent or significantly reduce graft rejection in bone marrow and organ transplantations and for use in the treatment of a wide variety of autoimmune diseases in humans and other mammals.
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公开(公告)号：US5192773A
公开(公告)日：1993-03-09
申请号：US547814
申请日：1990-07-02
IPC分类号： A61K31/34 , A61K31/16 , A61K31/165 , A61K31/341 , A61K31/343 , A61K31/357 , A61K31/36 , A61K31/38 , A61K31/381 , A61K31/395 , A61K31/40 , A61K31/401 , A61K31/4025 , A61K31/4427 , A61K31/443 , A61K31/4439 , A61K31/445 , A61K31/4525 , A61K31/453 , A61K31/454 , A61K31/4545 , A61P25/02 , A61P37/06 , C07C233/56 , C07C235/12 , C07C235/34 , C07D207/08 , C07D207/16 , C07D211/60 , C07D307/54 , C07D317/60 , C07D333/24 , C07D401/06 , C07D401/12 , C07D403/06 , C07D405/06 , C07D409/06
CPC分类号： C07D401/06 , C07C233/56 , C07C235/34 , C07D211/60 , C07D317/60 , C07D403/06 , C07D405/06 , Y10S514/885
摘要： This invention relates to a novel class of immunosuppressive compounds having an affinity for the FK-506 binding protein (FKBP). Once bound to this protein, the immunosuppressive compounds inhibit the prolyl peptidyl cis-trans isomerase (rotamase) activity of the FKBP and inhibit T cell activation. As such, the compounds of this invention can be used as immunosuppressive drugs to prevent or significantly reduce graft rejection in bone marrow and organ transplantations and for use in the treatment of a wide variety of autoimmune diseases in humans and other mammals.
摘要翻译： 本发明涉及对FK-506结合蛋白（FKBP）具有亲和力的新一类免疫抑制化合物。 一旦结合到该蛋白质上，免疫抑制化合物抑制FKBP的脯氨酰基顺式 - 反式异构酶（旋转异构酶）活性并抑制T细胞活化。 因此，本发明的化合物可用作免疫抑制药物，以预防或显着降低骨髓和器官移植中的移植排斥反应，并用于治疗人类和其他哺乳动物中各种自身免疫性疾病。
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公开(公告)号：US5622970A
公开(公告)日：1997-04-22
申请号：US456572
申请日：1995-06-01
IPC分类号： A61K31/34 , A61K31/16 , A61K31/165 , A61K31/341 , A61K31/343 , A61K31/357 , A61K31/36 , A61K31/38 , A61K31/381 , A61K31/395 , A61K31/40 , A61K31/401 , A61K31/4025 , A61K31/4427 , A61K31/443 , A61K31/4439 , A61K31/445 , A61K31/4525 , A61K31/453 , A61K31/454 , A61K31/4545 , A61P25/02 , A61P37/06 , C07C233/56 , C07C235/12 , C07C235/34 , C07D207/08 , C07D207/16 , C07D211/60 , C07D307/54 , C07D317/60 , C07D333/24 , C07D401/06 , C07D401/12 , C07D403/06 , C07D405/06 , C07D409/06
CPC分类号： C07D401/06 , C07C233/56 , C07C235/34 , C07D211/60 , C07D317/60 , C07D403/06 , C07D405/06 , Y10S514/885
摘要： This invention relates to a novel class of immunosuppressive compounds having an affinity for the FK-506 binding protein (FKBP). Once bound to this protein, the immunosuppressive compounds inhibit the prolyl peptidyl cis-trans isomerase (rotamase) activity of the FKBP and inhibit T cell activation. As such, the compounds of this invention can be used as immunosuppressive drugs to prevent or significantly reduce graft rejection in bone marrow and organ transplantations and for use in the treatment of a wide variety of autoimmune diseases in humans and other mammals.
摘要翻译： 本发明涉及对FK-506结合蛋白（FKBP）具有亲和力的新一类免疫抑制化合物。 一旦结合到该蛋白质上，免疫抑制化合物抑制FKBP的脯氨酰基顺式 - 反式异构酶（旋转异构酶）活性并抑制T细胞活化。 因此，本发明的化合物可用作免疫抑制药物，以预防或显着降低骨髓和器官移植中的移植排斥反应，并用于治疗人类和其他哺乳动物中各种自身免疫性疾病。
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公开(公告)号：US06541496B1
公开(公告)日：2003-04-01
申请号：US09556253
申请日：2000-04-24
申请人： David M. Armistead , Michael C. Badia , Guy W. Bemis , Randy S. Bethiel , Catharine A. Frank , Perry M. Novak , Steven M. Ronkin , Jeffrey O. Saunders
发明人： David M. Armistead , Michael C. Badia , Guy W. Bemis , Randy S. Bethiel , Catharine A. Frank , Perry M. Novak , Steven M. Ronkin , Jeffrey O. Saunders
IPC分类号： A61K3142
CPC分类号： C07D413/12 , A61K31/404 , A61K31/42 , A61K31/422 , C07C275/42 , C07D263/32 , Y02P20/55
摘要： The present invention relates to a novel class of compounds which inhibit IMPDH. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting IMPDH enzyme activity and consequently, may be advantageously used as therapeutic agents for IMPDH mediated processes. This invention also relates to methods for inhibiting the activity of IMPDH using the compounds of this invention and related compounds.
摘要翻译： 本发明涉及抑制IMPDH的新一类化合物。 本发明还涉及包含这些化合物的药物组合物。 本发明的化合物和药物组合物特别适用于抑制IMPDH酶活性，因此可有利地用作IMPDH介导的过程的治疗剂。 本发明还涉及使用本发明化合物和相关化合物抑制IMPDH活性的方法。
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公开(公告)号：US5932600A
公开(公告)日：1999-08-03
申请号：US816764
申请日：1997-03-14
申请人： Jeffrey O. Saunders , David M. Armistead , Michael C. Badia , Randy S. Bethiel , Catharine A. Frank , Doug Naegele , Perry M. Novak , David A. Pearlman , Steven M. Ronkin
发明人： Jeffrey O. Saunders , David M. Armistead , Michael C. Badia , Randy S. Bethiel , Catharine A. Frank , Doug Naegele , Perry M. Novak , David A. Pearlman , Steven M. Ronkin
IPC分类号： A61K31/4184 , A61K31/423 , A61K31/428 , C07D235/30 , C07D263/58 , C07D413/12 , C07D417/12 , A61K31/425 , A61K31/42
CPC分类号： C07D263/58 , A61K31/4184 , A61K31/423 , A61K31/428 , C07D235/30 , C07D413/12 , C07D417/12
摘要： The present invention relates to a novel class of compounds which are IMPDH inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting IMPDH enzyme activity and consequently, may be advantageously used as therapeutic agents for IMPDH mediated processes. This invention also relates to methods for inhibiting the activity of IMPDH using the compounds of this invention and related compounds.
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公开(公告)号：US6054472A
公开(公告)日：2000-04-25
申请号：US832165
申请日：1997-04-02
申请人： David M. Armistead , Michael C. Badia , Guy W. Bemis , Randy S. Bethiel , Catharine A. Frank , Perry M. Novak , Steven M. Ronkin , Jeffrey O. Saunders
发明人： David M. Armistead , Michael C. Badia , Guy W. Bemis , Randy S. Bethiel , Catharine A. Frank , Perry M. Novak , Steven M. Ronkin , Jeffrey O. Saunders
IPC分类号： A61K31/404 , A61K31/42 , A61K31/422 , C07C275/42 , C07D263/32 , C07D413/12 , A01N43/76 , C07D263/02 , C07D263/34
CPC分类号： C07D413/12 , A61K31/404 , A61K31/42 , A61K31/422 , C07C275/42 , C07D263/32
摘要： The present invention relates to a novel class of compounds which are IMPDH inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting IMPDH enzyme activity and consequently, may be advantageously used as therapeutic agents for IMPDH mediated processes. This invention also relates to methods for inhibiting the activity of IMPDH using the compounds of this invention and related compounds.
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