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公开(公告)号：US5204328A
公开(公告)日：1993-04-20
申请号：US789378
申请日：1991-11-05
摘要： Atrial natriuretic factor analogs containing N-alkylated amino acids and showing enhanced potency and increased metabolic stability. These analogs have natriuretic, diuretic and vasorelaxant activity, making them suitable for treating congestive heart failure and renal hypertension.
摘要翻译： 含有N-烷基化氨基酸的心房利钠因子类似物，显示出增强的效力和增加的代谢稳定性。 这些类似物具有利钠，利尿和血管舒张活性，使其适用于治疗充血性心力衰竭和肾性高血压。
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公开(公告)号：US5057603A
公开(公告)日：1991-10-15
申请号：US571803
申请日：1990-08-23
CPC分类号： C07K14/582 , A61K38/00
摘要： Novel peptides having potent natriuretic activity are disclosed with the following amino acid sequence: ##STR1## wherein X is L-Ile, D-Ile, D-allo-Ile, L-Met or D-Met, Y is Gly, L-Ala or D-Ala, A is optionally absent or is Ser, Ser-Ser, Arg-Ser-Ser, Arg-Arg-Ser-Ser, Leu-Arg-Arg-Ser-Ser or Ser-Leu-Arg-Arg-Ser-Ser and B is optionally absent or is Asn, Asn-Ser, Asn-Ser-Phe, Asn-Ser-Phe-Arg, or Asn-Ser-Phe-Arg-Tyr, provided that at least one of Y.sup.10, Y.sup.16, Y.sup.20 or Y.sup.22 is Ala or D-Ala, and the amides, lower alkyl esters and the physiologically acceptable metal salts and acid addition salts thereof.
摘要翻译： 公开了具有有效利钠肽活性的新肽，其具有以下氨基酸序列：其中X是L-Ile，D-Ile，D-allo-Ile，L-Met或D-Met，Y是Gly，L-Ala 或D-Ala，A任选不存在或是Ser，Ser-Ser，Arg-Ser-Ser，Arg-Arg-Ser-Ser，Leu-Arg-Arg-Ser-Ser或Ser-Leu-Arg-Arg-Ser -Ser和B任选不存在，或者是Asn，Asn-Ser，Asn-Ser-Phe，Asn-Ser-Phe-Arg或Asn-Ser-Phe-Arg-Tyr，条件是Y10，Y16， Y20或Y22是Ala或D-Ala，酰胺，低级烷基酯及其生理上可接受的金属盐和酸加成盐。
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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：US06248756B1
公开(公告)日：2001-06-19
申请号：US09248883
申请日：1999-02-11
申请人： Neville J. Anthony , Christopher Dinsmore , Robert P. Gomez , John H. Hutchinson , John S. Wai , Theresa M. Williams , Ian M. Bell , Mark W. Embrey , Thorsten E. Fisher
发明人： Neville J. Anthony , Christopher Dinsmore , Robert P. Gomez , John H. Hutchinson , John S. Wai , Theresa M. Williams , Ian M. Bell , Mark W. Embrey , Thorsten E. Fisher
IPC分类号： A61K314468
CPC分类号： C07D401/06 , C07D211/62 , C07D401/12 , C07D401/14 , C07D413/14
摘要： The present invention is directed to compounds which inhibit farnesyl-protein transferas (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.
摘要翻译： 本发明涉及抑制法尼基蛋白转移（Fatease-protein transferas，FTase）和致癌基因蛋白Ras的法呢基化的化合物。 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：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：US5972984A
公开(公告)日：1999-10-26
申请号：US960248
申请日：1997-10-29
申请人： Neville J. Anthony , Jeffrey M. Bergman , S. Jane deSolms , Chrisopher J. Dinsmore , Robert P. Gomez , Suzanne C. MacTough , Kelly M. Solinsky , Theresa M. Williams
发明人： Neville J. Anthony , Jeffrey M. Bergman , S. Jane deSolms , Chrisopher J. Dinsmore , Robert P. Gomez , Suzanne C. MacTough , Kelly M. Solinsky , Theresa M. Williams
IPC分类号： C07D233/54 , C07D401/14 , C07D403/06 , C07D403/02 , A61K31/40 , A61K31/415
CPC分类号： C07D233/64 , C07D401/14 , C07D403/06
摘要： The present invention comprises low molecular weight peptidyl compounds that inhibit the farnesyl-protein transferase. Furthermore, these compounds differ from the mono- or dipeptidyl analogs previously described as inhibitors of farnesyl-protein transferase in that they do not have a thiol moiety. The lack of the thiol offers unique advantages in terms of improved pharmacokinetic behavior in animals, prevention of thiol-dependent chemical reactions, such as rapid autoxidation and disulfide formation with endogenous thiols, and reduced systemic toxicity. Further contained in this invention are chemotherapeutic compositions containing these farnesyl transferase inhibitors and methods for their production.
摘要翻译： 本发明包括抑制法呢基蛋白转移酶的低分子量肽基化合物。 此外，这些化合物不同于先前描述为法呢基 - 蛋白转移酶抑制剂的单或二肽类似物，因为它们不具有硫醇部分。 缺乏硫醇在改善动物药代动力学行为方面提供独特的优势，防止硫醇依赖的化学反应，如快速自身氧化和内源性硫醇形成二硫键，并减少全身毒性。 本发明还包含含有这些法呢基转移酶抑制剂的化疗组合物及其生产方法。
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