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公开(公告)号:US5550251A
公开(公告)日:1996-08-27
申请号:US200320
申请日:1994-02-23
申请人: Ralph Hirschmann , Ellen Leahy , Paul Sprengeler
发明人: Ralph Hirschmann , Ellen Leahy , Paul Sprengeler
IPC分类号: C07D209/12 , C07D403/12 , A61K31/41
CPC分类号: C07D403/12 , C07D209/12
摘要: Compounds are provided which are crossreactive with peptides such as those bound by G-protein-linked receptors, together with preparative and therapeutic methods therefor. The compounds have the general structure: ##STR1## wherein at least one of R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 or R.sub.6 comprises a chemical functional group which causes the compounds to be crossreactive with the peptide of interest.
摘要翻译: 提供了与肽(例如由G蛋白连接的受体结合的肽)交联反应的化合物,以及其制备和治疗方法。 化合物具有以下通用结构:其中R 1,R 2,R 3,R 4,R 5或R 6中的至少一个包含使化合物与感兴趣肽交叉反应的化学官能团。
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公开(公告)号:US5250564A
公开(公告)日:1993-10-05
申请号:US806048
申请日:1991-12-12
申请人: Ralph Hirschmann , Ellen Leahy , Paul Sprengeler
发明人: Ralph Hirschmann , Ellen Leahy , Paul Sprengeler
IPC分类号: C07D209/12 , C07D209/14 , A61K31/40 , A61K31/405 , C07D209/04
CPC分类号: C07D209/12 , C07D209/14
摘要: Compounds are provided which are crossreactive with peptides such as those bound by G-protein-linked receptors, together with preparative and therapeutic methods therefor. The compounds have the general structure: ##STR1## wherein at least one of R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 or R.sub.6 comprises a chemical functional group which causes the compounds to be crossreactive with the peptide of interest.
摘要翻译: 提供了与肽(例如由G蛋白连接的受体结合的肽)交联反应的化合物,以及其制备和治疗方法。 化合物具有以下通用结构:其中R 1,R 2,R 3,R 4,R 5或R 6中的至少一个包含使化合物与感兴趣肽交叉反应的化学官能团。
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公开(公告)号:US5817879A
公开(公告)日:1998-10-06
申请号:US702811
申请日:1996-08-26
申请人: Ralph Hirschmann , Ellen Leahy , Paul Sprengeler
发明人: Ralph Hirschmann , Ellen Leahy , Paul Sprengeler
IPC分类号: C07D209/12 , C07D403/12 , C07C35/16 , C07D213/06 , C07D401/08
CPC分类号: C07D403/12 , C07D209/12
摘要: Compounds are provided which are crossreactive with peptides such as those bound by G-protein-linked receptors, together with preparative and therapeutic methods therefor. The compounds have the general structure: ##STR1## wherein at least one of R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 or R.sub.6 comprises a chemical functional group which causes the compounds to be crossreactive with the peptide of interest.
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公开(公告)号:US5489692A
公开(公告)日:1996-02-06
申请号:US18696
申请日:1993-02-17
申请人: Ralph Hirschmann , Amos B. Smith, III , Paul Sprengeler , Ryan C. Holcomb , Terence Keenan , John L. Wood , Mark Guzman
发明人: Ralph Hirschmann , Amos B. Smith, III , Paul Sprengeler , Ryan C. Holcomb , Terence Keenan , John L. Wood , Mark Guzman
IPC分类号: C07D207/36 , C07D207/38 , C07D207/00 , C07D413/00
CPC分类号: C07D207/38 , C07D207/36
摘要: Novel pyrrolinone-based compounds mimic or inhibit the biological and/or chemical activity of peptides, including peptide .beta.-strand conformations. Certain compounds contain functionalized pyrrolinone units in place of one or more amino acids of a target peptide.
摘要翻译: 新的基于吡咯啉酮的化合物模拟或抑制肽的生物和/或化学活性,包括肽β-链构象。 某些化合物含有官能化的吡咯啉酮单元代替目标肽的一个或多个氨基酸。
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公开(公告)号:US5811512A
公开(公告)日:1998-09-22
申请号:US588773
申请日:1996-01-19
CPC分类号: C07H15/18 , C07H15/04 , C07H15/26 , C07K14/6555 , A61K38/00
摘要: Compounds are provided which are crossreactive with peptides such as those which bind G-protein-linked receptors, together with preparative and therapeutic methods therefor.
摘要翻译: 提供了与肽结合反应的化合物,例如结合G蛋白连接的受体的那些,以及与其制备和治疗方法。
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公开(公告)号:US5552534A
公开(公告)日:1996-09-03
申请号:US144660
申请日:1993-10-28
申请人: Ralph F. Hirschmann , Kyriacos C. Nicolaou , Sherrie Pietranico , T. R. Reisine , Joseph M. Salvino , Paul Sprengeler , Catherine D. Strader
发明人: Ralph F. Hirschmann , Kyriacos C. Nicolaou , Sherrie Pietranico , T. R. Reisine , Joseph M. Salvino , Paul Sprengeler , Catherine D. Strader
摘要: Compounds are provided which are crossreactive with peptides such as those which bind G-protein-linked receptors, together with preparative and therapeutic methods therefor. The compounds have the general structure: ##STR1## wherein at least one of R.sub.1, R.sub.2, R.sub.3, R.sub.4, or R.sub.5 comprises a functional group which is chemically similar to that found in the peptide of interest.
摘要翻译: 提供了与肽结合反应的化合物,例如结合G蛋白连接的受体的那些,以及与其制备和治疗方法。 该化合物具有以下通用结构:其中R 1,R 2,R 3,R 4或R 5中的至少一个包含与目的肽中发现的化学相似的官能团。
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公开(公告)号:US5519060A
公开(公告)日:1996-05-21
申请号:US373564
申请日:1995-01-17
IPC分类号: A61K31/18 , A61K31/496 , A01N41/06 , A01N43/00 , A61K31/33
CPC分类号: A61K31/496 , A61K31/18
摘要: Methods are provided for using 2-hydroxy-3-aminopropylsulfonamides to mimic peptides and to modulate the chemical and/or biological activity of enzymes, particularly proteolytic enzymes. Also provided are compositions comprising the sulfonamides in admixture with a pharmaceutically acceptable carrier, adjuvant, or vehicle.
摘要翻译: 提供了使用2-羟基-3-氨基丙基磺酰胺模拟肽并调节酶,特别是蛋白水解酶的化学和/或生物活性的方法。 还提供了包含与药学上可接受的载体,佐剂或载体混合的磺酰胺的组合物。
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公开(公告)号:US5514814A
公开(公告)日:1996-05-07
申请号:US336371
申请日:1994-11-08
IPC分类号: C07D207/36 , C07D207/38 , C07D263/22 , C07D207/00
CPC分类号: C07D207/38 , C07D207/36 , C07D263/22
摘要: This invention relates to monomeric and polymeric pyrrolinone-based compounds, to the use of pyrrolinone-based compounds in place of amino acids in naturally-occurring or synthetic peptides, and to methods for preparing such compounds.
摘要翻译: 本发明涉及使用基于吡咯烷酮的化合物代替天然存在的或合成的肽中的氨基酸的基于单体和聚合的吡咯烷酮的化合物以及制备这些化合物的方法。
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公开(公告)号:US20050026929A1
公开(公告)日:2005-02-03
申请号:US10421372
申请日:2003-04-23
申请人: Sui Cai , Ben Cebon , Joane Litvak , Keith Pararajasingham , Emma Shelton , Jeffrey Spencer , David Sperandio , Paul Sprengeler , Vincent Tai , Robert Yee
发明人: Sui Cai , Ben Cebon , Joane Litvak , Keith Pararajasingham , Emma Shelton , Jeffrey Spencer , David Sperandio , Paul Sprengeler , Vincent Tai , Robert Yee
IPC分类号: A61P35/00 , C07D231/14 , C07D233/90 , C07D263/34 , C07D271/06 , C07D277/56 , C07D401/06 , C07D403/06 , C07D409/12 , C07D409/14 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/06 , C07D417/12 , C07D453/06 , C07D471/08 , C07D491/04 , C07D491/10 , C07D417/02 , A61K31/422 , A61K31/427 , A61K31/454 , A61K31/496 , C07D413/02 , C07
CPC分类号: C07D263/34 , C07D231/14 , C07D271/06 , C07D277/56 , C07D401/06 , C07D403/06 , C07D409/12 , C07D409/14 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/06 , C07D417/12 , C07D453/06 , C07D471/08 , C07D491/04 , C07D491/10
摘要: The present invention related to certain phenyl derivatives that are activators of caspases and inducers of apoptosis, pharmaceutical composition comprising these compounds and method of treating cancer utilizing these compounds.
摘要翻译: 本发明涉及作为胱天蛋白酶的活化剂和凋亡诱导剂的某些苯基衍生物,包含这些化合物的药物组合物和利用这些化合物治疗癌症的方法。
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公开(公告)号:US06455570B1
公开(公告)日:2002-09-24
申请号:US09973493
申请日:2001-10-09
IPC分类号: A61K3140
CPC分类号: C07D207/36
摘要: A compound of the formula wherein: R1, R2, R3, R4, R5, R6 are as defined herein, useful for the inhibition of inhibition of matrix metalloproteases (MMPs)and for treating conditions mediated by elevated levels of MMPs such as osteoarthritis, rheumatoid arthritis, septic arthritis, periodontal disease, gingivitis, solid tumor growth and tumor invasion by secondary metastasis, corneal ulceration, dermal ulceration, epidermolysis bullosa, neural degeneration, multiple sclerosis and surgical wound healing.
摘要翻译: 方解石的化合物:R1,R2,R3,R4,R5,R6如本文所定义,可用于抑制基质金属蛋白酶(MMPs)的抑制和用于治疗由升高的MMP水平介导的病症,例如骨关节炎,类风湿性关节炎 脓毒性关节炎,牙周病,牙龈炎,实体肿瘤生长和继发性转移肿瘤侵袭,角膜溃疡,皮肤溃疡,大疱性表皮松解,神经变性,多发性硬化和手术伤口愈合。
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