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公开(公告)号：US20100113421A1
公开(公告)日：2010-05-06
申请号：US12444014
申请日：2007-10-02
IPC分类号： A61K31/55 , C07D207/00 , A61K31/40 , C07D401/12 , A61K31/454 , C07D495/04
CPC分类号： C07D207/36 , C07D401/06 , C07D401/12 , C07D403/12 , C07D409/12 , C07D495/04
摘要： Compounds of Formula (I) are HIV reverse transcriptase inhibitors, wherein X, R1, R2, R3, R4 and R5 are defined herein. The compounds of Formula (I) and their pharmaceutically acceptable salts are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset or progression, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
摘要翻译： 式（I）化合物是HIV逆转录酶抑制剂，其中X，R 1，R 2，R 3，R 4和R 5在本文中定义。 式（I）化合物及其药学上可接受的盐可用于HIV逆转录酶的抑制，艾滋病毒感染的预防和治疗以及预防，延缓发作或进展以及治疗艾滋病。 化合物及其盐可以用作药物组合物中的成分，任选与其它抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。
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公开(公告)号：US07659264B2
公开(公告)日：2010-02-09
申请号：US11664905
申请日：2005-10-05
IPC分类号： C07D403/12 , C07D403/14 , A61K31/55
CPC分类号： C07D491/20 , C07D471/10 , C07D471/20 , C07D491/10
摘要： The present invention is directed to compounds of Formula I: Formula I: I and Formula II: (where variables R1, R2, R3, R4, A, B, J, Q, T, V, W, X and Y are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
摘要翻译： 本发明涉及式I化合物：式I：I和式II（其中变量R1，R2，R3，R4，A，B，J，Q，T，V，W，X和Y如上所定义 可用作CGRP受体的拮抗剂，可用于治疗或预防涉及CGRP的疾病，例如头痛，偏头痛和丛集性头痛。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及CGRP的疾病中的用途。
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公开(公告)号：US07534784B2
公开(公告)日：2009-05-19
申请号：US12082233
申请日：2008-04-09
申请人： Christopher S. Burgey , Zhengwu J. Deng , Diem N. Nguyen , Daniel V. Paone , Anthony W. Shaw , Theresa M. Williams
发明人： Christopher S. Burgey , Zhengwu J. Deng , Diem N. Nguyen , Daniel V. Paone , Anthony W. Shaw , Theresa M. Williams
IPC分类号： C07D401/14 , A61K31/55 , A61P25/06
CPC分类号： C07D487/04 , C07D471/04
摘要： The present invention is directed to compounds of Formula I: (where variables R1, R2, R3, R4, A, B, G, J, Q, T, U, V, W, X and Y are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
摘要翻译： 本发明涉及式I化合物（其中变量R1，R2，R3，R4，A，B，G，J，Q，T，U，V，W，X和Y如本文所定义） CGRP受体的拮抗剂，可用于治疗或预防涉及CGRP的疾病，如头痛，偏头痛和丛集性头痛。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及CGRP的疾病中的用途。
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公开(公告)号：US07452903B2
公开(公告)日：2008-11-18
申请号：US11724066
申请日：2007-03-14
申请人： Christopher S. Burgey , Diem N. Nguyen , Daniel V. Paone , Anthony W. Shaw , Theresa M. Williams
发明人： Christopher S. Burgey , Diem N. Nguyen , Daniel V. Paone , Anthony W. Shaw , Theresa M. Williams
IPC分类号： C07D471/02 , C07D513/02 , A61K31/44 , A61P25/06
CPC分类号： C07D487/04 , C07D471/04
摘要： The present invention is directed to compounds of Formula I: and Formula II: (where variables R1, R2, R3, R4, A, B, G, J, Q, T, U, V, W, X and Y are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
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公开(公告)号：US06333335B1
公开(公告)日：2001-12-25
申请号：US09609205
申请日：2000-06-30
IPC分类号： A61K31437
CPC分类号： C07D471/04
摘要： The present invention is directed to tetrahydro-imidazopyridinyl compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.
摘要翻译： 本发明涉及抑制异戊烯基 - 蛋白质转移酶和癌基因蛋白Ras的异戊烯化的四氢 - 咪唑并吡啶基化合物。 本发明还涉及含有本发明化合物的化疗组合物和抑制异戊烯基 - 蛋白质转移酶和癌基因蛋白Ras的异戊烯化的方法。
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公开(公告)号：US5977134A
公开(公告)日：1999-11-02
申请号：US985320
申请日：1997-12-04
申请人： Terrence M. Ciccarone , Wasyl Halczenko , John H. Hutchinson , William C. Lumma, Jr. , Gerald E. Stokker , Craig A. Stump , Theresa M. Williams
发明人： Terrence M. Ciccarone , Wasyl Halczenko , John H. Hutchinson , William C. Lumma, Jr. , Gerald E. Stokker , Craig A. Stump , Theresa M. Williams
IPC分类号： C07D235/30 , C07D401/06 , C07D403/06 , C07D471/04 , C07D401/02 , A61K31/415 , A61K31/47
CPC分类号： C07D401/06 , C07D235/30 , C07D403/06 , C07D471/04
摘要： The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
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公开(公告)号：US5631280A
公开(公告)日：1997-05-20
申请号：US448865
申请日：1995-05-24
申请人： Terrence M. Ciccarone , Christopher J. Dinsmore , Gerald E. Stokker , John S. Wai , Theresa M. Williams
发明人： Terrence M. Ciccarone , Christopher J. Dinsmore , Gerald E. Stokker , John S. Wai , Theresa M. Williams
IPC分类号： C07D521/00 , A61K31/135 , A61K31/165 , A61K31/40 , A61K31/403 , A61K31/4035 , A61K31/404 , A61P35/00 , A61P43/00 , C07C323/25 , C07C323/60 , C07D209/08 , C07D209/46 , C07D209/44
CPC分类号： C07C323/25 , C07C323/60 , C07D209/08 , C07D209/46 , C07C2102/10
摘要： The present invention comprises peptidomimetic compounds which comprise a suitably aniline and aminoalkylbenzene moieties. The instant compounds inhibit the farnesyl-protein transferase enzyme and the farnesylation of certain proteins. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
摘要翻译： 本发明包括含有合适的苯胺和氨基烷基苯部分的拟肽化合物。 本发明化合物抑制法呢基蛋白转移酶和某些蛋白质的法呢基化。 本发明进一步涉及含有本发明化合物的化疗组合物和抑制法呢基蛋白转移酶的方法和癌基因蛋白Ras的法呢基化。
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公开(公告)号：US5527819A
公开(公告)日：1996-06-18
申请号：US488957
申请日：1995-06-07
申请人： Theresa M. Williams , Terrence M. Ciccarone , Walfred S. Saari , John S. Wai , William J. Greenlee , Suresh K. Balani , Mark E. Goldman , Anthony D. Theoharides, deceased , Jacob M. Hoffman, Jr. , William C. Lumma, Jr. , Joel R. Huff , Clarence S. Rooney , Philip E. Sanderson
发明人： Theresa M. Williams , Terrence M. Ciccarone , Walfred S. Saari , John S. Wai , William J. Greenlee , Suresh K. Balani , Mark E. Goldman , Anthony D. Theoharides, deceased , Jacob M. Hoffman, Jr. , William C. Lumma, Jr. , Joel R. Huff , Clarence S. Rooney , Philip E. Sanderson
IPC分类号： C07D209/12 , C07D209/30 , C07D209/42 , C07D401/06 , C07D401/12 , C07D403/12 , C07D405/06 , C07D405/12 , C07D413/06 , C07D417/12 , C07D521/00 , A61K31/40
CPC分类号： C07D231/12 , C07D209/12 , C07D209/30 , C07D209/42 , C07D233/56 , C07D249/08 , C07D401/06 , C07D401/12 , C07D403/12 , C07D405/06 , C07D405/12 , C07D413/06 , C07D417/12
摘要： Novel indole compounds inhibit HIV reverse transcriptase, and are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, anti-infectives, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.
摘要翻译： 新型吲哚化合物抑制HIV逆转录酶，可用于预防或治疗艾滋病毒和艾滋病感染，作为化合物，药学上可接受的盐，药物组合物成分，无论是否与其他抗病毒药物结合使用，抗感染药物 ，免疫调节剂，抗生素或疫苗。 还描述了治疗艾滋病的方法和预防或治疗HIV感染的方法。
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公开(公告)号：US07632832B2
公开(公告)日：2009-12-15
申请号：US11795678
申请日：2006-01-13
IPC分类号： C07D401/14 , A61K31/4745 , A61P25/06
CPC分类号： C07D401/14
摘要： Compounds of Formula I: (where variables R1, R2, R3, R7, G, J, Q, T, W, X and Y are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache, and pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
摘要翻译： 式I化合物（其中变量R1，R2，R3，R7，G，J，Q，T，W，X和Y如本文所定义）可用作CGRP受体的拮抗剂，可用于治疗或预防 CGRP涉及，如头痛，偏头痛和丛集性头痛，以及包含这些化合物的药物组合物，以及这些化合物和组合物在预防或治疗CGRP所涉及的疾病中的用途。
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公开(公告)号：US07390798B2
公开(公告)日：2008-06-24
申请号：US11660798
申请日：2005-02-09
IPC分类号： C07D401/14 , C07D471/10 , A61K31/553 , A61K31/55 , A61K31/438 , A61K31/4166 , A61P25/06
CPC分类号： C07D471/04 , C07D401/12 , C07D413/12 , C07D519/00
摘要： The present invention is directed to compounds of Formula I: I (where variables A1, A2, B, J, K, m, n, R4, R5a, R5b and R5c are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved
摘要翻译： 本发明涉及式I的化合物：I（其中变量A 1，A 2，B，J，K，m，n，R 4 R 5c，R 5b和R 5c如本文所定义）可用作CGRP受体的拮抗剂并且可用于治疗 或预防CGRP所涉及的疾病，如头痛，偏头痛和丛集性头痛。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及CGRP的疾病中的用途
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