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1.发明授权1-pyrimidinylacetamide compounds which are inhibitors of human leukocyte elastase 失效作为人白细胞弹性蛋白酶抑制剂的1-嘧啶基乙酰胺化合物
公开(公告)号：US5736535A
公开(公告)日：1998-04-07
申请号：US375136
申请日：1995-01-19
申请人： Peter Robert Bernstein , Philip Duke Edwards , Andrew Shaw , Ashokkumar Bhikkappa Shenvi , Royston Martin Thomas , Chris Allan Veale , Peter Warner , Donald John Wolanin
发明人： Peter Robert Bernstein , Philip Duke Edwards , Andrew Shaw , Ashokkumar Bhikkappa Shenvi , Royston Martin Thomas , Chris Allan Veale , Peter Warner , Donald John Wolanin
IPC分类号： A61K38/55 , A61K38/00 , A61P7/02 , A61P9/00 , A61P9/08 , A61P9/10 , A61P9/12 , A61P11/00 , A61P29/00 , C07K5/06 , A61K31/69 , C07F5/02 , C07F5/04
CPC分类号： C07K5/06191 , A61K38/00
摘要： The present invention relates to certain novel substituted derivatives which are 1-pyrimidinylacetamide derivatives of formula I, ##STR1## which are inhibitors of human leukocyte elastase (HLE), also known as human neutrophil elastase (HNE), making them useful whenever such inhibition is desired, such as for research tools in pharmacological, diagnostic and related studies and in the treatment of diseases in mammals in which HLE is implicated. The invention also includes intermediates useful in the synthesis of these substituted derivatives, processes for preparing the substituted derivatives, pharmaceutical compositions containing such substituted derivatives and methods for their use.
摘要翻译： 本发明涉及作为人白细胞弹性蛋白酶（HLE）抑制剂（也称为人嗜中性粒细胞弹性蛋白酶（HNE））的式I的1-嘧啶基乙酰胺衍生物的某些新的取代衍生物，使其在这种抑制 是期望的，例如在药理学，诊断和相关研究中的研究工具以及涉及HLE的哺乳动物的疾病的治疗。 本发明还包括可用于合成这些取代衍生物的中间体，制备取代衍生物的方法，含有这种取代的衍生物的药物组合物及其使用方法。
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公开(公告)号：US5721222A
公开(公告)日：1998-02-24
申请号：US519651
申请日：1995-08-25
申请人： Peter Robert Bernstein , Andrew Shaw , Royston Martin Thomas , Chris Allan Veale , Peter Warner , Donald John Wolanin
发明人： Peter Robert Bernstein , Andrew Shaw , Royston Martin Thomas , Chris Allan Veale , Peter Warner , Donald John Wolanin
IPC分类号： A61K38/55 , A61K38/00 , A61P7/02 , A61P9/00 , A61P9/08 , A61P9/10 , A61P9/12 , A61P11/00 , A61P29/00 , C07K5/02 , C07K5/06 , C07K5/078 , C07K5/08 , C07D211/84 , A61K31/44 , C07D213/81 , C07D401/12
CPC分类号： C07K5/06191 , C07K5/0205 , C07K5/06139 , A61K38/00
摘要： The present invention relates to certain novel heterocyclic ketones which are 1-pyridylacetamide ketones of formula I, set out herein, which are inhibitors of human leukocyte elastase (HLE), also known as human neutrophil elastase (HNE), making them useful whenever such inhibition is desired, such as for research tools in pharmacological, diagnostic and related studies and in the treatment of diseases in mammals in which HLE is implicated. The invention also includes intermediates useful in the synthesis of these heterocyclic ketones, processes for preparing the heterocyclic ketones, pharmaceutical compositions containing such heterocyclic ketones and methods for their use.
摘要翻译： 本发明涉及作为人类白细胞弹性蛋白酶（HLE）抑制剂（也称为人嗜中性粒细胞弹性蛋白酶（HNE））的本文列出的作为式I的1-吡啶基乙酰胺酮的某些新型杂环酮，只要这种抑制 是期望的，例如在药理学，诊断和相关研究中的研究工具以及涉及HLE的哺乳动物的疾病的治疗。 本发明还包括可用于合成这些杂环酮的中间体，制备杂环酮的方法，含有该杂环酮的药物组合物及其使用方法。
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公开(公告)号：US5686628A
公开(公告)日：1997-11-11
申请号：US595692
申请日：1996-02-02
IPC分类号： A61K38/55 , A61K38/00 , A61K38/06 , A61P9/10 , A61P11/00 , A61P11/10 , A61P29/00 , C07C213/02 , C07C215/08 , C07K1/02 , C07K1/14 , C07K5/06 , C07K5/062 , C07K5/083 , C07D207/323
CPC分类号： C07K5/06191 , A61K38/00
摘要： The present invention relates to particular forms of a novel 1-substituted-N-�2-methyl-1-(trifluoroacetyl)propyl!pyrrolidine-2-carboxamide which are inhibitors of human leukocyte elastase (HLE), also known as human neutrophil elastase (HNE), making them useful whenever such inhibition is desired, such as for research tools in pharmacological, diagnostic and related studies and in the treatment of diseases in mammals in which HLE is implicated. The invention also includes pharmaceutical compositions containing such forms, processes for preparing the forms and intermediates useful in the synthesis of the forms.
摘要翻译： 本发明涉及作为人类白细胞弹性蛋白酶（HLE）抑制剂的新型1-取代-N- [2-甲基-1-（三氟乙酰基）丙基]吡咯烷-2-甲酰胺的具体形式，也称为人嗜中性粒细胞弹性蛋白酶 （HNE），使其在需要这种抑制时有用，例如用于药理学，诊断和相关研究中的研究工具以及涉及HLE的哺乳动物的疾病的治疗。 本发明还包括含有这种形式的药物组合物，用于制备可用于合成形式的形式和中间体的方法。
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公开(公告)号：US6048889A
公开(公告)日：2000-04-11
申请号：US274572
申请日：1999-03-23
IPC分类号： A61K38/55 , A61K38/00 , A61K38/06 , A61P9/10 , A61P11/00 , A61P11/10 , A61P29/00 , C07C213/02 , C07C215/08 , C07K1/02 , C07K1/14 , C07K5/06 , C07K5/062 , C07K5/083 , A61K31/40 , C07D207/323
CPC分类号： C07K5/06191 , A61K38/00
摘要： The present invention relates to particular forms of a novel 1-substituted-N-[2-methyl-1-(trifluoroacetyl)propyl]pyrrolidine-2-carboxamide which are inhibitors of human leukocyte elastase (HLE), also known as human neutrophil elastase (HNE), making them useful whenever such inhibition is desired, such as for research tools in pharmacological, diagnostic and related studies and in the treatment of diseases in mammals in which HLE is implicated. The invention also includes pharmaceutical compositions containing such forms, processes for preparing the forms and intermediates useful in the synthesis of the forms.
摘要翻译： 本发明涉及作为人类白细胞弹性蛋白酶（HLE）抑制剂的新型1-取代-N- [2-甲基-1-（三氟乙酰基）丙基]吡咯烷-2-甲酰胺的具体形式，也称为人嗜中性粒细胞弹性蛋白酶 （HNE），使其在需要这种抑制时有用，例如用于药理学，诊断和相关研究中的研究工具以及涉及HLE的哺乳动物的疾病的治疗。 本发明还包括含有这种形式的药物组合物，用于制备可用于合成形式的形式和中间体的方法。
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公开(公告)号：US6054593A
公开(公告)日：2000-04-25
申请号：US100735
申请日：1998-06-19
IPC分类号： A61K38/55 , A61K38/00 , A61K38/06 , A61P9/10 , A61P11/00 , A61P11/10 , A61P29/00 , C07C213/02 , C07C215/08 , C07K1/02 , C07K1/14 , C07K5/06 , C07K5/062 , C07K5/083 , C07D207/16
CPC分类号： C07K5/06191 , A61K38/00
摘要： The present invention relates to particular forms of a novel 1-substituted-N-[2-methyl-1-(trifluoroacetyl)propyl]pyrrolidine-2-carboxamide which are inhibitors of human leukocyte elastase (HLE), also known as human neutrophil elastase (HNE), making them useful whenever such inhibition is desired, such as for research tools in pharmacological, diagnostic and related studies and in the treatment of diseases in mammals in which HLE is implicated. The invention also includes pharmaceutical compositions containing such forms, processes for preparing the forms and intermediates useful in the synthesis of the forms.
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公开(公告)号：US5808097A
公开(公告)日：1998-09-15
申请号：US918626
申请日：1997-08-22
IPC分类号： A61K38/55 , A61K38/00 , A61K38/06 , A61P9/10 , A61P11/00 , A61P11/10 , A61P29/00 , C07C213/02 , C07C215/08 , C07K1/02 , C07K1/14 , C07K5/06 , C07K5/062 , C07K5/083 , C07D207/323
CPC分类号： C07K5/06191 , A61K38/00
摘要： The present invention relates to particular forms of a novel 1-substituted-N-�2-methyl-1-(trifluoroacetyl)propyl!pyrrolidine-2-carboxamide which are inhibitors of human leukocyte elastase (HLE), also known as human neutrophil elastase (HNE), making them useful whenever such inhibition is desired, such as for research tools in pharmacological, diagnostic and related studies and in the treatment of diseases in mammals in which HLE is implicated. The invention also includes pharmaceutical compositions containing such forms, processes for preparing the forms and intermediates useful in the synthesis of the forms.
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公开(公告)号：US5965576A
公开(公告)日：1999-10-12
申请号：US980399
申请日：1997-11-26
申请人： Ashokkumar Bhikkappa Shenvi , Robert Toms Jacobs , Scott Carson Miller , Cyrus John Ohnmacht, Jr. , Chris Allan Veale
发明人： Ashokkumar Bhikkappa Shenvi , Robert Toms Jacobs , Scott Carson Miller , Cyrus John Ohnmacht, Jr. , Chris Allan Veale
IPC分类号： A61K31/40 , A61P11/00 , C07D401/06 , C07D401/14 , A61K31/445
CPC分类号： C07D401/06 , C07D401/14
摘要： Compounds of formula I ##STR1## wherein Q.sup.1, Q.sup.2, Q.sup.3, and Q.sup.4 have any of the meanings given in the specification, their N-oxides, and their pharmaceutically acceptable salts are nonpeptide antagonists of neurokinin A and useful for the treatment of asthma, etc. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.
摘要翻译： 其中Q1，Q2，Q3和Q4具有本说明书中给出的任何含义，其N-氧化物及其药学上可接受的盐的式I化合物是神经激肽A的非肽拮抗剂，可用于治疗哮喘等。另外 公开的是药物组合物，制备式I化合物的方法和中间体。
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8.发明授权Diastereomeric pure trifluoromethyl ketone peptide derivatives as inhibitors of human leukocyte elastase 失效非对映体纯三氟甲基酮肽衍生物作为人白细胞弹性蛋白酶抑制剂
公开(公告)号：US5907043A
公开(公告)日：1999-05-25
申请号：US13853
申请日：1998-01-27
IPC分类号： A61K38/00 , A61K20060101 , A61P9/00 , A61P11/00 , A61P29/00 , C07K20060101 , C07K1/02 , C07K5/06 , C07K5/062 , C07K5/083 , C07D207/12 , C07C229/48
CPC分类号： C07K5/06052 , C07K5/06191 , A61K38/00
摘要： The present invention relates to pyrrolidine derivatives, and more particularly to the compound (S)-1-�(S)-2-(4-methoxybenzamido)-3-methylbutyryl!-N-�(S)-2-methyl-1-(trifluoroacetyl)propyl!pyrrolidine-2-carboxamide, shown by formula I, and solvates thereof. The present invention also provides pharmaceutical compositions, intermediates and methods of preparation of the compound. The compound of formula I is an inhibitor of human neutrophil elastase and is useful in the treatment of diseases in which the enzyme is implicated, such as, for example, emphysema and acute respiratory distress syndrome (ARDS).
摘要翻译： 本发明涉及吡咯烷衍生物，特别是涉及化合物（S）-1 - [（S）-2-（4-甲氧基苯甲酰氨基）-3-甲基丁酰基] -N - [（S）-2-甲基-1 - （三氟乙酰基）丙基]吡咯烷-2-甲酰胺，及其溶剂合物。 本发明还提供药物组合物，中间体和化合物的制备方法。 式I化合物是人中性粒细胞弹性蛋白酶的抑制剂，可用于治疗涉及该酶的疾病，例如肺气肿和急性呼吸窘迫综合征（ARDS）。
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9.发明授权Substituted piperidinobutyl nitrogen-containing heterocyclic compounds and analogues thereof as neurokinin antagonists 失效取代的哌啶丁基含氮杂环化合物及其类似物作为神经激肽拮抗剂
公开(公告)号：US5739149A
公开(公告)日：1998-04-14
申请号：US790867
申请日：1997-02-03
申请人： Robert Toms Jacobs , Scott Carson Miller , Ashokkumar Bhikkappa Shenvi , Cyrus John Ohnmacht, Jr. , Chris Allan Veale
发明人： Robert Toms Jacobs , Scott Carson Miller , Ashokkumar Bhikkappa Shenvi , Cyrus John Ohnmacht, Jr. , Chris Allan Veale
IPC分类号： A61K31/4427 , A61K31/445 , A61K31/505 , A61P11/00 , A61P11/06 , A61P43/00 , C07D401/06 , C07D401/14 , C07D401/04
CPC分类号： C07D401/06 , C07D401/14
摘要： Compounds of formula I ##STR1## wherein Q.sup.1, Q.sup.2, Q.sup.3, and Q.sup.4 have any of the meanings given in the specification, their N-oxides, and their pharmaceutically acceptable salts are nonpeptide antagonists of neurokinin A and useful for the treatment of asthma, etc. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.
摘要翻译： 式I的化合物其中Q1，Q2，Q3和Q4具有本说明书中给出的任何含义，其N-氧化物及其药学上可接受的盐是神经激肽A的非肽拮抗剂，可用于治疗 哮喘等。还公开了药物组合物，制备式I化合物的方法和中间体。
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10.发明授权Diastereomeric pure trifluoromethyl ketone peptide derivatives as inhibitors of human leukocyte elastase 失效非对映体纯三氟甲基酮肽衍生物作为人白细胞弹性蛋白酶抑制剂
公开(公告)号：US6037363A
公开(公告)日：2000-03-14
申请号：US253659
申请日：1999-02-22
IPC分类号： A61K38/00 , A61K20060101 , A61P9/00 , A61P11/00 , A61P29/00 , C07K20060101 , C07K1/02 , C07K5/06 , C07K5/062 , C07K5/083 , A61K31/40 , C07D207/12
CPC分类号： C07K5/06052 , C07K5/06191 , A61K38/00
摘要： The present invention relates to pyrrolidine derivative compounds, and more particularly to the compound (S)-1-[(S)-2-(4-methoxybenzamido)-3-methylbutyryl]-N-[(S)-2-methyl-1-(trifluoroacetyl)propyl]pyrrolidine-2-carboxamide, shown by the formula I, a pharmaceutical composition comprising this compound in a crystalline form and a process for preparing the pharmaceutical composition. The compound of formula I is an inhibitor of human neutrophil elastase and is useful in the treatment of diseases in which the enzyme is implicated, such as, for example, emphysema and acute respiratory distress syndrome (ARDS).
摘要翻译： 本发明涉及吡咯烷衍生物化合物，更具体地说，涉及化合物（S）-1 - [（S）-2-（4-甲氧基苯甲酰氨基）-3-甲基丁酰基] -N - [（S）-2-甲基 - 1-（三氟乙酰基）丙基]吡咯烷-2-甲酰胺，由式I表示，包含结晶形式的该化合物的药物组合物和制备该药物组合物的方法。 式I化合物是人中性粒细胞弹性蛋白酶的抑制剂，可用于治疗涉及该酶的疾病，例如肺气肿和急性呼吸窘迫综合征（ARDS）。
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