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1. 发明授权

US5731413A Method of synthesis of peptidyl aldehydes 失效
标题翻译：肽基醛合成方法
公开(公告)号：US5731413A
公开(公告)日：1998-03-24
申请号：US482281
申请日：1995-06-07
申请人： Thomas Roy Webb , John Eugene Reiner , Susan Yoshiko Tamura , William Charles Ripka , Raymond Dagnino, Jr. , Ruth Foelsche Nutt
发明人： Thomas Roy Webb , John Eugene Reiner , Susan Yoshiko Tamura , William Charles Ripka , Raymond Dagnino, Jr. , Ruth Foelsche Nutt
IPC分类号： A61K31/445 , A61K38/00 , A61P43/00 , C07D207/16 , C07D211/56 , C07D401/12 , C07K1/10 , C07K5/06 , C07K5/072 , C07K5/08 , C07K5/00
CPC分类号： C07D401/12 , C07D207/16 , C07D211/56 , C07K5/0606 , C07K5/06113 , A61K38/00
摘要： This invention provides solution-phase and solid-phase methods for the synthesis of peptidyl argininals and to �novel! reagents useful therein.
摘要翻译：本发明提供了用于合成肽基精氨酸的溶液相和固相方法及其中有用的[新颖]试剂。

2. 发明授权

US06500948B1 Metalloproteinase inhibitors-compositions, uses preparation and intermediates thereof 失效
标题翻译：金属蛋白酶抑制剂 - 其组合物，用途，制备及其中间体
公开(公告)号：US06500948B1
公开(公告)日：2002-12-31
申请号：US09675555
申请日：2000-09-29
申请人： Scott E. Zook , Raymond Dagnino, Jr. , Michael E. Deason , Steven L. Bender , Michael J. Melnick
发明人： Scott E. Zook , Raymond Dagnino, Jr. , Michael E. Deason , Steven L. Bender , Michael J. Melnick
IPC分类号： C07D41700
CPC分类号： C07D401/12 , C07D239/04 , C07D241/04 , C07D279/12 , C07D417/12
摘要： The invention relates to compounds of the formula 1: wherein: Z is O or S; V is a divalent radical which together with C* and N forms a ring having six ring atoms, where each of said ring atoms other than C* and N independently is unsubstituted or substituted by a suitable substituent, and at least one of said other ring atoms is a heteroatom selected from O, N and S, and the remainder are carbon atoms; and Ar is an aryl or heteroaryl group; and pharmaceutically acceptable prodrugs, salts and solvates thereof. The invention further relates to pharmaceutically acceptable prodrugs, salts and solvates of these compounds. The invention also relates to methods of inhibiting the activity of metalloproteinases by administering a compound of the formula I or a prodrug, salt of solvate thereof. The invention further relates to pharmaceutical compositions comprising an effective amount of these compounds, prodrugs, salts, and solvates. The invention still further relates to methods and intermediates useful for preparing these compounds, prodrugs, salts, and solvates.
摘要翻译：本发明涉及式1化合物：其中：Z为O或S; V是与C *和N一起形成具有六个环原子的环的二价基团，其中除C *和N之外的所述环原子各自独立地是未取代的或被合适的取代基取代，并且所述另一个环中的至少一个原子是选自O，N和S的杂原子，其余为碳原子; Ar为芳基或杂芳基; 其药学上可接受的前药，其盐和溶剂化物。本发明还涉及这些化合物的药学上可接受的前药，盐和溶剂化物。本发明还涉及通过给予式I化合物或其前药，其溶剂合物的盐来抑制金属蛋白酶的活性的方法。本发明还涉及包含有效量的这些化合物，前药，盐和溶剂合物的药物组合物。本发明还涉及可用于制备这些化合物，前药，盐和溶剂合物的方法和中间体。

3. 发明授权

US6153757A Metalloproteinase inhibitors and intermediates useful for their preparation 失效
标题翻译：金属蛋白酶抑制剂和中间体可用于制备
公开(公告)号：US6153757A
公开(公告)日：2000-11-28
申请号：US11971
申请日：1998-06-29
申请人： Scott E. Zook , Raymond Dagnino, Jr. , Michael E. Deason , Steven L. Bender , Michael J. Melnick
发明人： Scott E. Zook , Raymond Dagnino, Jr. , Michael E. Deason , Steven L. Bender , Michael J. Melnick
IPC分类号： C07D241/04 , A61K31/00 , A61K31/44 , A61K31/4409 , A61K31/4427 , A61K31/495 , A61K31/50 , A61K31/535 , A61K31/5375 , A61K31/54 , A61K31/541 , A61P19/02 , A61P29/00 , A61P35/00 , A61P35/04 , A61P43/00 , C07C309/28 , C07D20060101 , C07D213/62 , C07D213/68 , C07D213/70 , C07D213/89 , C07D233/54 , C07D233/64 , C07D239/04 , C07D249/08 , C07D265/30 , C07D277/62 , C07D279/00 , C07D279/12 , C07D295/00 , C07D307/38 , C07D401/00 , C07D401/12 , C07D403/12 , C07D413/00 , C07D413/12 , C07D417/00 , C07D417/12 , C07F7/18
CPC分类号： C07D265/30 , C07D239/04 , C07D241/04 , C07D279/12 , C07D401/12 , C07D417/12
摘要： The invention relates to compounds of formula (1) ##STR1## wherein: Z is O or S; V is a divalent radical which together with C* and N forms a ring having six ring atoms, where each of said ring atoms other than C* and N independently is unsubstituted or substituted by a suitable substituent, and at least one of said other ring atoms is a heteroatom selected from O, N and S, and the remainder is carbon atoms; and Ar is an aryl or heteroaryl group; and pharmaceutically acceptable prodrugs, salts and solvates thereof. The invention further relates to pharmaceutically acceptable prodrugs, salts and solvates of these compounds. The invention also relates to methods of inhibiting the activity of metalloproteinases by administering a compound of formula (1) or a prodrug, salt or solvate thereof. The invention further relates to pharmaceutical compositions comprising an effective amount of these compounds, prodrugs, salts, and solvates. The invention still further relates to methods and intermediates useful for preparing these compounds, prodrugs, salts, and solvates.
摘要翻译： PCT No.PCT / US96 / 19328 Sec。 371日期1998年6月29日第 102（e）日期1998年6月29日PCT 1996年12月5日PCT公布。出版物WO97 / 20824 日期：1997年6月12日本发明涉及式（1）化合物，其中：Z为O或S; V是与C *和N一起形成具有六个环原子的环的二价基团，其中除C *和N之外的所述环原子各自独立地是未取代的或被合适的取代基取代，并且所述另一个环中的至少一个原子是选自O，N和S的杂原子，其余为碳原子; Ar为芳基或杂芳基; 及其药学上可接受的前药，其盐和溶剂化物。本发明还涉及这些化合物的药学上可接受的前药，盐和溶剂化物。本发明还涉及通过给予式（1）化合物或其前药，盐或溶剂化物来抑制金属蛋白酶活性的方法。本发明还涉及包含有效量的这些化合物，前药，盐和溶剂合物的药物组合物。本发明还涉及可用于制备这些化合物，前药，盐和溶剂合物的方法和中间体。

4. 发明授权

US06774243B2 Efficient synthetic routes for the preparation of rhinovirus protease inhibitors and key intermediates 失效
标题翻译：用于制备鼻病毒蛋白酶抑制剂和关键中间体的高效合成路线
公开(公告)号：US06774243B2
公开(公告)日：2004-08-10
申请号：US09984555
申请日：2001-10-30
申请人： Qingping Tian , Naresh K. Nayyar , Srinivasan Babu , Junhua Tao , Terence Jarold Moran , Raymond Dagnino, Jr. , Lennert J. Mitchell, Jr. , Travis Paul Remarchuk , Michael Joseph Melnick , Steven Lee Bender
发明人： Qingping Tian , Naresh K. Nayyar , Srinivasan Babu , Junhua Tao , Terence Jarold Moran , Raymond Dagnino, Jr. , Lennert J. Mitchell, Jr. , Travis Paul Remarchuk , Michael Joseph Melnick , Steven Lee Bender
IPC分类号： C07D20726
CPC分类号： B01J19/2435 , B01J19/2475 , B01J2219/00033 , B01J2219/00099 , B01J2219/00103 , B01J2219/00159 , B01J2219/00162 , B01J2219/00177 , C07B2200/07 , C07C69/732 , C07C229/34 , C07C271/22 , C07C303/28 , C07D207/26 , C07D261/18 , C07D413/12 , C07C309/65
摘要： Efficient synthetic routes for the preparation of rhinovirus protease inhibitors of formula I, as well as key intermediates useful in those synthetic routes. These compounds of formula I, as well as pharmaceutical compositions that contain these compounds, are suitable for treating patients or hosts infected with one or more picornaviruses.
摘要翻译：用于制备式I的鼻病毒蛋白酶抑制剂的高效合成路线，以及在那些合成路线中有用的关键中间体。这些式I化合物以及含有这些化合物的药物组合物适用于治疗患有一种或多种微小核糖核酸病毒感染的患者或宿主。

5. 发明授权

US06355807B1 Efficient synthetic routes for the preparation of rhinovirus protease inhibitors and key intermediates 失效
标题翻译：用于制备鼻病毒蛋白酶抑制剂和关键中间体的高效合成路线
公开(公告)号：US06355807B1
公开(公告)日：2002-03-12
申请号：US09643864
申请日：2000-08-23
申请人： Qingping Tian , Naresh K. Nayyar , Srinivasan Babu , Junhua Tao , Terence Jarold Moran , Raymond Dagnino, Jr. , Lennert J. Mitchell, Jr. , Travis Paul Remarchuk , Michael Joseph Melnick , Steven Lee Bender
发明人： Qingping Tian , Naresh K. Nayyar , Srinivasan Babu , Junhua Tao , Terence Jarold Moran , Raymond Dagnino, Jr. , Lennert J. Mitchell, Jr. , Travis Paul Remarchuk , Michael Joseph Melnick , Steven Lee Bender
IPC分类号： C07D20726
CPC分类号： C07D207/26 , B01J19/2435 , B01J19/2475 , B01J2219/00033 , B01J2219/00099 , B01J2219/00103 , B01J2219/00159 , B01J2219/00162 , B01J2219/00177 , C07B2200/07 , C07C69/732 , C07C229/34 , C07C271/22 , C07C303/28 , C07D261/18 , C07D413/12 , C07C309/65
摘要： Efficient synthetic routes for the preparation of rhinovirus protease inhibitors of formula I, as well as key intermediates useful in those synthetic routes. These compounds of formula I, as well as pharmaceutical compositions that contain these compounds, are suitable for treating patients or hosts infected with one or more picornaviruses
摘要翻译：用于制备式I的鼻病毒蛋白酶抑制剂的高效合成途径，以及在那些合成路线中有用的关键中间体。这些式I化合物以及含有这些化合物的药物组合物适用于治疗感染了一种或多种微小核糖核酸病毒的患者或宿主

6. 发明授权

US06849732B2 Metalloproteinase inhibitors, pharmaceutical compositions containing them and their pharmaceutical uses, and methods and intermediates useful for their preparation 失效
标题翻译：金属蛋白酶抑制剂，含有它们的药物组合物及其药物用途，以及可用于其制备的方法和中间体
公开(公告)号：US06849732B2
公开(公告)日：2005-02-01
申请号：US10298842
申请日：2002-11-18
申请人： Scott E. Zook , Raymond Dagnino, Jr. , Michael E. Deason , Steven L. Bender , Michael J. Melnick
发明人： Scott E. Zook , Raymond Dagnino, Jr. , Michael E. Deason , Steven L. Bender , Michael J. Melnick
IPC分类号： C07D239/04 , C07D241/04 , C07D279/12 , C07D401/12 , C07D417/12
CPC分类号： C07D401/12 , C07D239/04 , C07D241/04 , C07D279/12 , C07D417/12
摘要： The invention relates to compounds of the formula 1: wherein: Z is O or S; V is a divalent radical which together with C* and N forms a ring having six ring atoms, where each of said ring atoms other than C* and N independently is unsubstituted or substituted by a suitable substituent, and at least one of said other ring atoms is a heteroatom selected from O, N and S, and the remainder are carbon atoms; and Ar is an aryl or heteroaryl group; and pharmaceutically acceptable prodrugs, salts and solvates thereof. The invention further relates to pharmaceutically acceptable prodrugs, salts and solvates of these compounds. The invention also relates to methods of inhibiting the activity of metalloproteinases by administering a compound of the formula I or a prodrug, salt or solvate thereof. The invention further relates to pharmaceutical compositions comprising an effective amount of these compounds, prodrugs, salts, and solvates. The invention still further relates to methods and intermediates useful for preparing these compounds, prodrugs, salts, and solvates.
摘要翻译：本发明涉及式1化合物：其中：Z为O或S; V是与C *和N一起形成具有六个环原子的环的二价基团，其中除C *和N之外的所述环原子各自独立地是未取代的或被合适的取代基取代，并且所述另一个环中的至少一个原子是选自O，N和S的杂原子，其余为碳原子; Ar为芳基或杂芳基; 及其药学上可接受的前药，其盐和溶剂化物。本发明还涉及这些化合物的药学上可接受的前药，盐和溶剂化物。本发明还涉及通过给予式I化合物或其前药，盐或溶剂化物来抑制金属蛋白酶活性的方法。本发明还涉及包含有效量的这些化合物，前药，盐和溶剂合物的药物组合物。本发明还涉及可用于制备这些化合物，前药，盐和溶剂合物的方法和中间体。

7. 发明授权

US5514777A Methods of synthesis of peptidyl argininals 失效
标题翻译：肽基精氨酸合成方法
公开(公告)号：US5514777A
公开(公告)日：1996-05-07
申请号：US261380
申请日：1994-06-17
申请人： Thomas R. Webb , John E. Reiner , Susan Y. Tamura , William C. Ripka , Raymond Dagnino, Jr.
发明人： Thomas R. Webb , John E. Reiner , Susan Y. Tamura , William C. Ripka , Raymond Dagnino, Jr.
IPC分类号： A61K31/445 , A61K38/00 , A61P43/00 , C07D207/16 , C07D211/56 , C07D401/12 , C07K1/10 , C07K5/06 , C07K5/072 , C07K5/08 , C07K5/00 , C07D211/22 , C07K7/00 , C07K17/00
CPC分类号： C07D401/12 , C07D207/16 , C07D211/56 , C07K5/0606 , C07K5/06113 , A61K38/00
摘要： This invention provides solution-phase methods for the synthesis of peptidyl argininals and to novel reagents useful therein.
摘要翻译：本发明提供了用于合成肽基精氨酸的溶液相方法及其中有用的新型试剂。

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