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1. 发明授权

US5254558A Substituted 1,3-diazines as leukocyte elastase inhibitors 失效
标题翻译：取代的1,3-二嗪作为白细胞弹性蛋白酶抑制剂
公开(公告)号：US5254558A
公开(公告)日：1993-10-19
申请号：US930568
申请日：1992-08-14
申请人： Peter R. Bernstein , Philip D. Edwards , Royston M. Thomas , Chris A. Veale , Peter Warner , Donald J. Wolanin
发明人： Peter R. Bernstein , Philip D. Edwards , Royston M. Thomas , Chris A. Veale , Peter Warner , Donald J. Wolanin
IPC分类号： A61K31/505 , A61K38/00 , A61P9/00 , A61P9/10 , A61P9/12 , A61P11/00 , A61P29/00 , C07D239/46 , C07D239/47 , C07D401/04 , C07D401/12 , C07D401/14 , C07D409/04 , C07D409/14 , C07K5/06 , C07K5/08 , C07D239/22
CPC分类号： C07D239/47 , C07D401/04 , C07D401/12 , C07D401/14 , C07D409/04 , C07D409/14 , C07K5/06191 , A61K38/00
摘要： The present invention relates to certain novel substituted heterocycles which are 1-pyrimidinylacetamide compounds 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 substituted heterocycles, processes for preparing the substituted heterocycles, pharmaceutical compositions containing such substituted heterocycles and methods for their use.

2. 发明授权

US5532366A Heterocyclic amides 失效
标题翻译：杂环酰胺
公开(公告)号：US5532366A
公开(公告)日：1996-07-02
申请号：US375201
申请日：1995-01-19
申请人： Philip D. Edwards , Peter Warner , Donald J. Wolanin
发明人： Philip D. Edwards , Peter Warner , Donald J. Wolanin
IPC分类号： A61K38/00 , A61P7/02 , A61P9/08 , A61P9/10 , A61P9/12 , A61P11/00 , A61P29/00 , A61P43/00 , C07K1/113 , C07K5/06 , C07K5/078 , C07K14/81 , A61K31/505 , C07D471/04
CPC分类号： C07K5/06191 , A61K38/00
摘要： The present invention relates to certain novel amide derivatives which are pyrido[3,4-d]pyrimidin-7-ylacetamides 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 amide derivatives, processes for preparing the amide derivatives, pharmaceutical compositions containing such amide derivatives 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））的吡啶并[3,4-d]嘧啶-7-基乙酰胺的某些新型酰胺衍生物，需要抑制，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酰胺衍生物的中间体，制备酰胺衍生物的方法，含有这种酰胺衍生物的药物组合物及其使用方法。

3. 发明授权

US5441960A 1-pyrimidinylacetamide human leukocyte elastate inhibitors 失效
标题翻译： 1-嘧啶基乙酰胺人类白细胞弹性蛋白酶抑制剂
公开(公告)号：US5441960A
公开(公告)日：1995-08-15
申请号：US44866
申请日：1993-04-08
申请人： Peter R. Bernstein , Philip D. Edwards , Andrew Shaw , Royston M. Thomas , Chris A. Veale , Peter Warner , Donald J. Wolanin
发明人： Peter R. Bernstein , Philip D. Edwards , Andrew Shaw , Royston M. Thomas , Chris A. Veale , Peter Warner , Donald J. 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 , C07K5/08 , A61K31/505 , C07D239/22
CPC分类号： C07K5/0205 , C07K5/06191 , A61K38/00
摘要： The present invention relates to certain novel substituted ketones which are 1-pyrimidinylacetamide derivatives of formula I, ##STR1## 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 ##STR2## useful in the synthesis of these substituted ketones processes for preparing the substituted ketones pharmaceutical compositions containing such substituted ketones 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所示的1-嘧啶基乙酰胺衍生物的某些新的取代酮，其为如果需要这种抑制作用，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中是有用的。本发明还包括可用于合成这些取代酮的中间体制备含取代酮的取代酮的药物组合物的方法及其使用方法。

4. 发明授权

US4910190A Peptide derivatives 失效
标题翻译：肽衍生物
公开(公告)号：US4910190A
公开(公告)日：1990-03-20
申请号：US5538
申请日：1987-01-20
申请人： Scott H. Bergeson , Philip D. Edwards , John A. Schwartz , Andrew Shaw , Mark M. Stein , Diane A. Trainor , Richard A. Wildonger , Donald J. Wolanin
发明人： Scott H. Bergeson , Philip D. Edwards , John A. Schwartz , Andrew Shaw , Mark M. Stein , Diane A. Trainor , Richard A. Wildonger , Donald J. Wolanin
IPC分类号： A61K31/40 , A61K31/401 , A61K31/4025 , A61K31/44 , A61K31/4409 , A61K31/4418 , A61K31/4427 , A61K31/4433 , A61K31/535 , A61K38/00 , A61K38/55 , A61P9/10 , A61P11/00 , A61P29/00 , A61P43/00 , C07C205/02 , C07C205/26 , C07C205/43 , C07D207/16 , C07D213/26 , C07D333/00 , C07D401/12 , C07D403/12 , C07D409/12 , C07K1/113 , C07K5/04 , C07K5/06 , C07K5/08 , C07K5/093 , C07K14/81 , C12N9/99
CPC分类号： C07C205/26 , C07C205/02 , C07C205/43 , C07K5/06191 , C07K5/0819 , C07K5/0827 , A61K38/00
摘要： The invention concerns pharmaceutically useful trifluoromethyl ketone substituted di-, tri- and tetra-peptide derivatives of the formulae Ia, Ib, Ic set out hereinafter, and salts thereof, which are inhibitors of human leukocyte elastase. Also described herein are pharmaceutical compositions containing a peptide derivative and processes and intermediates for use in the manufacture of the peptide derivatives.
摘要翻译：本发明涉及作为人白细胞弹性蛋白酶抑制剂的药学上有用的三氟甲基酮取代的下式Ia，Ib和Ic的二，三和四肽衍生物及其盐。本文还描述了含有肽衍生物的药物组合物和用于制备肽衍生物的方法和中间体。

5. 发明授权

US5486529A Certain pyridyl ketones for treating diseases involving leukocyte elastase 失效
标题翻译：某些用于治疗涉及白细胞弹性蛋白酶的疾病的吡啶酮
公开(公告)号：US5486529A
公开(公告)日：1996-01-23
申请号：US45496
申请日：1993-04-08
申请人： Peter R. Bernstein , Andrew Shaw , Royston M. Thomas , Chris A. Veale , Peter Warner , Donald J. Wolanin
发明人： Peter R. Bernstein , Andrew Shaw , Royston M. Thomas , Chris A. Veale , Peter Warner , Donald J. 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 , A61K31/44 , C07D211/84 , 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。

6. 发明授权

US5521179A Heterocyclic amides 失效
标题翻译：杂环酰胺
公开(公告)号：US5521179A
公开(公告)日：1996-05-28
申请号：US045009
申请日：1993-04-08
申请人： Peter R. Bernstein , Andrew Shaw , Royston M. Thomas , Peter Warner , Donald J. Wolanin
发明人： Peter R. Bernstein , Andrew Shaw , Royston M. Thomas , Peter Warner , Donald J. Wolanin
IPC分类号： A61K38/00 , C07K5/06 , C07D237/00 , C07D211/72 , C07D215/14 , C07D401/00
CPC分类号： C07K5/06191 , A61K38/00
摘要： The present invention relates to certain novel heterocyclic amides which are 1-pyridylacetamide compounds 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 amides, processes for preparing the heterocyclic amides, pharmaceutical compositions containing such heterocyclic amides and methods for their use.
摘要翻译：本发明涉及某些新颖的杂环酰胺，它们是本文列出的式I的1-吡啶基乙酰胺化合物，其是人类白细胞弹性蛋白酶（HLE）的抑制剂，也被称为人嗜中性粒细胞弹性蛋白酶（HNE）），使得它们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杂环酰胺的中间体，制备杂环酰胺的方法，含有这种杂环酰胺的药物组合物及其使用方法。

7. 发明授权

US5405852A Amide derivatives 失效
标题翻译：酰胺衍生物
公开(公告)号：US5405852A
公开(公告)日：1995-04-11
申请号：US71624
申请日：1993-06-03
申请人： Chris A. Veale , Peter Warner , Donald J. Wolanin
发明人： Chris A. Veale , Peter Warner , Donald J. Wolanin
IPC分类号： A61K38/55 , A61K38/00 , A61P29/00 , C07K1/113 , C07K5/06 , C07K5/078 , A61K31/44 , C07D471/06
CPC分类号： C07K5/06139 , A61K38/00
摘要： The present invention relates to certain novel amide ##STR1## derivatives which are pyrido[3,4-b]indol-2-ylacetamides 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 amide derivatives, processes for preparing the amide derivatives, pharmaceutical compositions containing such amide 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））的吡啶并[3,4-b]吲哚-2-基乙酰胺的某些新颖的酰胺I型衍生物如果需要这种抑制，它们是有用的，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酰胺衍生物的中间体，制备酰胺衍生物的方法，含有这种酰胺衍生物的药物组合物及其使用方法。

8. 发明授权

US5270301A Fluoro-amide derivatives 失效
标题翻译：氟 - 酰胺衍生物
公开(公告)号：US5270301A
公开(公告)日：1993-12-14
申请号：US519618
申请日：1990-05-07
申请人： Donald J. Wolanin
发明人： Donald J. Wolanin
IPC分类号： A61K38/00 , A61P11/00 , A61P43/00 , C07C237/22 , C07K1/02 , C07K1/06 , C07K1/113 , C07K5/02 , C07K5/06 , C07K5/08 , C07K5/083 , A61K37/02 , A61K31/34 , A61K31/38 , A61K31/44 , A61K31/505 , C07D213/06 , C07D213/46 , C07D239/02 , C07D307/02 , C07D317/44
CPC分类号： C07K5/0205 , C07K5/06191 , A61K38/00
摘要： The present invention relates to certain fluoro-amide derivatives, as described herein, which are human leukocyte elastase (HLE) inhibitors 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, including treatment of tissue degenerative diseases such as pulmonary emphysema. The invention also includes intermediates useful in the synthesis of these fluoro-amide derivatives, processes for preparing them, pharmaceutical compositions containing such peptide derivatives and methods for their use.

9. 发明授权

US06218431B1 Substituted biphenyls 失效
标题翻译：取代的联苯
公开(公告)号：US06218431B1
公开(公告)日：2001-04-17
申请号：US08904119
申请日：1997-07-31
申请人： William R. Schoen , Gaetan H. Ladouceur , James H. Cook, II , Timothy G. Lease , Donald J. Wolanin , Richard H. Kramss , Donald L. Hertzog , Martin H. Osterhout
发明人： William R. Schoen , Gaetan H. Ladouceur , James H. Cook, II , Timothy G. Lease , Donald J. Wolanin , Richard H. Kramss , Donald L. Hertzog , Martin H. Osterhout
IPC分类号： A61K31275
CPC分类号： C07D213/30 , C07D213/32 , C07D213/34 , C07D213/38 , C07D213/50 , C07D213/55 , C07D213/64 , C07D213/70 , C07D213/74 , C07D213/80 , C07D215/14 , C07D221/04 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/06 , C07D401/12 , C07D405/04 , C07D405/06 , C07D405/12 , C07D409/04 , C07D411/12 , C07D413/06 , C07D413/12 , C07D417/12 , C07D487/04 , C07F7/1804
摘要： Substituted biphenyls having glucagon receptor antagonistic activity. Claimed compounds have the formula wherein R1a and R1b independently represent (C1-C6) alkyl; R2 represents (C1-C10) alkyl or substituted (C1-C10) alkyl wherein the substituents are independently from 1 to 3 of —SR7; R7 represents phenyl, or substituted phenyl wherein the substituents are independently 1-5 of halogen, trifluoromethyl, (C1-C6) alkyl, (C1-C6) alkoxy, nitro, cyano, or hydroxyl; R3 represents substituted (C1-C6) alkyl wherein the substituents are 1-2 hydroxyl groups; G represents a substituent selected from the group consisting of halogen, (C1-C6) alkyl, and OR4 wherein R4 is H or (C1-C6) alkyl; and y is 0 or an integer of 1-3. Pharmaceutical compositions containing such compounds and methods of treatment of glucagon-mediated conditions by administering such compounds are also claimed.
摘要翻译：具有胰高血糖素受体拮抗活性的取代的联苯。权利要求的化合物具有R1a和R1b独立地表示（C1-C6）烷基; R2代表（C1-C10）烷基或取代的（C1-C10）烷基，其中取代基独立地为1至3的-SR7; R7代表苯基或取代苯基，其中取代基独立地为1-5个卤素，三氟甲基，（C1-C6）烷基，（C1-C6）烷氧基，硝基，氰基或羟基; R3表示取代基（C1-C6）烷基，其中取代基是1-2个羟基; G表示选自卤素，（C1-C6）烷基和OR4的取代基，其中R4是H或（C1-C6）烷基; y为0或1-3的整数。还要求保护含有这些化合物的药物组合物和通过施用这些化合物治疗胰高血糖素介导的病症的方法。

10. 发明授权

US5804581A Inhibition of matrix metalloproteases by substituted phenalkyl compounds 失效
标题翻译：通过取代的苯烷基化合物抑制基质金属蛋白酶
公开(公告)号：US5804581A
公开(公告)日：1998-09-08
申请号：US856696
申请日：1997-05-15
申请人： Donald J. Wolanin
发明人： Donald J. Wolanin
IPC分类号： A61K31/165 , C07C59/84 , C07C235/84 , C07D295/192 , A61K31/195 , A61K31/535 , C07D295/13
CPC分类号： C07D295/192 , A61K31/165 , A61K31/5375 , C07C235/84 , C07C59/84
摘要： Matrix metalloprotease inhibiting compounds, pharmaceutical compositions thereof and a method of disease treatment using such compounds are presented. The compounds of the invention have the generalized formula: ##STR1## wherein T is a substituent and R.sup.24 is a substituted amide moiety. These compounds are useful for inhibiting matrix metalloproteases and, therefore, combating conditions to which MMP's contribute, such as osteoarthritis, rheumatoid arthritis, septic arthritis, periodontal disease, corneal ulceration, proteinuria, aneurysmal aortic disease, dystrophobic epidermolysis, bullosa, conditions leading to inflammatory responses, osteopenias mediated by MMP activity, tempera mandibular joint disease, demyelating diseases of the nervous system, tumor metastasis or degenerative cartilage loss following traumatic joint injury, and coronary thrombosis from athrosclerotic plaque rupture. The present invention also provides pharmaceutical compositions and methods for treating such conditions.
摘要翻译：提出了基质金属蛋白酶抑制化合物，其药物组合物和使用这些化合物的疾病治疗方法。本发明的化合物具有以下通式：其中T是取代基，R24是取代的酰胺部分。这些化合物可用于抑制基质金属蛋白酶，因此可用于抗MMP的作用，例如骨关节炎，类风湿性关节炎，脓毒性关节炎，牙周病，角膜溃疡，蛋白尿，动脉瘤性主动脉疾病，疏水性表皮松解症，大疱疹，导致炎症的病症反应，由MMP活性介导的骨质减少，颞下颌关节疾病，神经系统脱髓鞘疾病，创伤性关节损伤后的肿瘤转移或退行性软骨损失，以及来自动脉粥样硬化斑块破裂的冠状动脉血栓形成。本发明还提供了用于治疗这些病症的药物组合物和方法。

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