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1. 发明授权

US5364850A Substituted tyrosyl diamide compounds 失效
标题翻译：取代的酪氨酰二酰胺化合物
公开(公告)号：US5364850A
公开(公告)日：1994-11-15
申请号：US125897
申请日：1993-09-24
申请人： Donald W. Hansen, Jr. , Nizal S. Chandrakumar , Karen B. Peterson , Sofya Tsymbalov , Robert K. Husa
发明人： Donald W. Hansen, Jr. , Nizal S. Chandrakumar , Karen B. Peterson , Sofya Tsymbalov , Robert K. Husa
IPC分类号： C07C233/47 , C07C237/20 , C07C237/22 , C07C271/20 , C07C271/22 , C07C275/16 , C07C311/58 , C07D207/14 , C07D295/185 , A61K31/495 , A61K31/165 , A61K31/40 , C07D241/04
CPC分类号： C07D295/185 , C07C233/47 , C07C237/20 , C07C237/22 , C07C271/20 , C07C271/22 , C07C275/16 , C07C311/58 , C07D207/14
摘要： The present invention provides substituted tyrosyl diamide compounds of general Formula I: ##STR1## and the pharmaceutically-acceptable salts thereof, which are useful for inducing analgesia in animals, pharmaceutical compositions comprising a pharmaceutically-acceptable carrier and a compound of Formula I, and a method for inducing analgesia in an animal in need thereof comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.
摘要翻译：本发明提供通式I的取代的酪氨酰二酰胺化合物：式I及其药学上可接受的盐，其可用于诱导动物镇痛，药物组合物包含药学上可接受的载体和式I化合物，以及用于在有需要的动物中诱导镇痛的方法，包括向动物施用治疗有效量的式I化合物。

2. 发明授权

US5272175A Substituted tyrosyl diamide compounds 失效
标题翻译：取代的酪氨酰二酰胺化合物
公开(公告)号：US5272175A
公开(公告)日：1993-12-21
申请号：US886276
申请日：1992-05-20
申请人： Donald W. Hansen, Jr. , Nizal S. Chandrakumar , Karen B. Peterson , Sofya Tsymbalov , Robert K. Husa
发明人： Donald W. Hansen, Jr. , Nizal S. Chandrakumar , Karen B. Peterson , Sofya Tsymbalov , Robert K. Husa
IPC分类号： C07C233/47 , C07C237/20 , C07C237/22 , C07C271/20 , C07C271/22 , C07C275/16 , C07C311/58 , C07D207/14 , C07D295/185 , A61K31/165 , A61K31/17 , A61K31/325 , C07C237/28
CPC分类号： C07D295/185 , C07C233/47 , C07C237/20 , C07C237/22 , C07C271/20 , C07C271/22 , C07C275/16 , C07C311/58 , C07D207/14
摘要： The present invention provides substituted tyrosyl diamide compounds of general Formula I: ##STR1## and the pharmaceutically-acceptable salts thereof, which are useful for inducing analgesia in animals, pharmaceutical compositions comprising a pharmaceutically-acceptable carrier and a compound of Formula I, and a method for inducing analgesia in an animal in need thereof comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.
摘要翻译：本发明提供通式I的取代的酪氨酰二酰胺化合物：式I及其药学上可接受的盐，其可用于诱导动物镇痛，药物组合物包含药学上可接受的载体和式I化合物，以及用于在有需要的动物中诱导镇痛的方法，包括向动物施用治疗有效量的式I化合物。

3. 发明授权

US5389645A Substituted tyrosyl diamine amide compounds 失效
标题翻译：取代的酪氨酰二胺酰胺化合物
公开(公告)号：US5389645A
公开(公告)日：1995-02-14
申请号：US929275
申请日：1992-08-13
申请人： Donald W. Hansen, Jr. , Nizal S. Chandrakumar , Karen B. Peterson , Sofya Tsymbalov
发明人： Donald W. Hansen, Jr. , Nizal S. Chandrakumar , Karen B. Peterson , Sofya Tsymbalov
IPC分类号： C07C237/20 , C07C271/20 , C07C271/28 , C07C275/24 , C07D207/16 , C07D215/48 , C07D295/185 , A61K31/47
CPC分类号： C07D295/185 , C07C237/20 , C07C271/20 , C07C271/28 , C07C275/24 , C07D207/16 , C07D215/48
摘要： The present invention provides substituted tyrosyl diamine amide compounds of general Formula I: ##STR1## and the pharmaceutically-acceptable salts thereof, which are useful for inducing analgesia in animals, pharmaceutical compositions comprising a pharmaceutically-acceptable carrier and a compound of Formula I, and a method for inducing analgesia in an animal in need thereof comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.
摘要翻译：本发明提供通式I的取代的酪氨酰二胺酰胺化合物：式I及其药学上可接受的盐，其可用于诱导动物镇痛，药物组合物包含药学上可接受的载体和式I化合物以及在有需要的动物中诱导镇痛的方法，包括向动物施用治疗有效量的式I化合物。

4. 发明授权

US5169833A Substituted cyclic pentapeptides 失效
标题翻译：取代的环状五肽
公开(公告)号：US5169833A
公开(公告)日：1992-12-08
申请号：US703524
申请日：1991-05-21
申请人： Donald W. Hansen, Jr. , Sofya Tsymbalov , Nizal S. Chandrakumar , Donna L. Hammond , Henry I. Mosberg
发明人： Donald W. Hansen, Jr. , Sofya Tsymbalov , Nizal S. Chandrakumar , Donna L. Hammond , Henry I. Mosberg
IPC分类号： A61K38/00 , C07K14/70
CPC分类号： C07K14/702 , A61K38/00 , Y10S514/809
摘要： The present invention provides substituted cyclic pentapeptide compounds of general Formula I: ##STR1## and the pharmaceutically-acceptable slats, esters and amides thereof, which are useful for inducing analgesia in animals, pharmaceutical compositions comprising a pharmaceutically-acceptable carrier and a compound of Formula I, and a method for inducing analgesia in an animal in need thereof comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.
摘要翻译：本发明提供通式I的取代的环状五肽化合物：式I及其药学上可接受的片，酯和酰胺，其可用于诱导动物镇痛，药物组合物包含药学上可接受的载体和化合物的式I化合物，以及在有需要的动物中诱导镇痛的方法，包括向动物施用治疗有效量的式I化合物。

5. 发明授权

US5360796A Imidazo[1,2-a]pyridinylalkyl phosphonic acid compounds for treatment of neurotoxic injury 失效
标题翻译：咪唑并[1,2-a]吡啶基烷基膦酸化合物，用于治疗神经毒性损伤
公开(公告)号：US5360796A
公开(公告)日：1994-11-01
申请号：US871995
申请日：1991-12-09
申请人： Donald W. Hansen, Jr. , Gilbert W. Adelstein , Karen B. Peterson , Sofya Tsymbalov
发明人： Donald W. Hansen, Jr. , Gilbert W. Adelstein , Karen B. Peterson , Sofya Tsymbalov
IPC分类号： C07D471/04 , C07F9/6561 , A61K31/44
CPC分类号： C07D471/04 , C07F9/6561
摘要： A class of imidazo[1,2-a]pyridinylalkyl phosphonic acid compounds is described for treatment to reduce neurotoxic injury associated with anoxia or ischemia which typically follows stroke, cardiac arrest or perinatal asphyxia. The treatment includes administration of a compound of this class alone or in a composition in an amount effective as an antagonist to inhibit excitotoxic actions at major neuronal excitatory amino acid receptor sites. Compounds of most interest are those of the formula: ##STR1## and the carboxylic and phosphonic alkyl esters and salts thereof; wherein the substituents are defined herein.
摘要翻译：描述了一类咪唑并[1,2-a]吡啶基烷基膦酸化合物用于治疗以减少与缺氧或缺血相关的神经毒性损伤，其通常在中风，心脏骤停或围产期窒息之后。治疗包括单独施用该类化合物或以有效作为拮抗剂的量的组合物施用以抑制主要神经元兴奋性氨基酸受体位点的兴奋性毒性作用。最感兴趣的化合物是下式的化合物：其中羧酸和膦酸烷基酯及其盐; 其中取代基在本文中定义。

6. 发明授权

US5633237A Imidazo[1,2-a]pyridinylalkyl phosphonic acid compounds for treatment of neurotoxic injury 失效
标题翻译：咪唑并[1,2-a]吡啶基烷基膦酸化合物，用于治疗神经毒性损伤
公开(公告)号：US5633237A
公开(公告)日：1997-05-27
申请号：US271395
申请日：1994-07-06
申请人： Donald W. Hansen, Jr. , Gilbert W. Adelstein , Karen B. Peterson , Sofya Tsymbalov
发明人： Donald W. Hansen, Jr. , Gilbert W. Adelstein , Karen B. Peterson , Sofya Tsymbalov
IPC分类号： C07D471/04 , C07F9/6561 , A61K31/44
CPC分类号： C07D471/04 , C07F9/6561
摘要： A class of imidazo[1,2-a]pyridinylalkyl phosphonic acid compounds is described for treatment to reduce neurotoxic injury associated with anoxia or ischemia which typically follows stroke, cardiac arrest or perinatal asphyxia. The treatment includes administration of a compound of this class alone or in a composition in an amount effective as an antagonist to inhibit excitotoxic actions at major neuronal excitatory amino acid receptor sites. Compounds of most interest are those of the formula: ##STR1## and the carboxylic and phosphonic alkyl esters and salts thereof; wherein R.sup.9 is selected from hydrido, methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl and cycloheptyl; wherein each of Y.sub.m and Y.sub.n is a spacer group independently selected methylene and ethylene radicals which may be unsubstituted and from methylene radicals which may be substituted with a group selected from halo, hydroxy and oxo;wherein each of m and n is a number independently selected from zero to two, inclusive; wherein each X and T is one or more groups independently selected from hydrido, alkyl, cycloalkyl, halo, haloalkyl, hydroxy, hydroxyalkyl, alkoxy, alkoxyalkyl and alkanoyl; or a pharmaceutically-acceptable acid addition salt thereof.
摘要翻译：描述了一类咪唑并[1,2-a]吡啶基烷基膦酸化合物用于治疗以减少与缺氧或缺血相关的神经毒性损伤，其通常在中风，心脏骤停或围产期窒息之后。治疗包括单独施用该类化合物或以有效作为拮抗剂的量的组合物施用以抑制主要神经元兴奋性氨基酸受体位点的兴奋性毒性作用。最感兴趣的化合物是下式的化合物：其中羧酸和膦酸烷基酯及其盐; 其中R 9选自氢，甲基，乙基，正丙基，异丙基，正丁基，异丁基，仲丁基，叔丁基，环丙基，环丁基，环戊基，环己基和环庚基; 其中Ym和Yn各自是间隔基团，独立地选择亚甲基和亚乙基，其可以是未取代的，可以被可以被选自卤素，羟基和氧代的基团取代的亚甲基; 其中m和n各自独立地选自0至2，包括0和2; 其中每个X和T是一个或多个独立地选自氢，烷基，环烷基，卤素，卤代烷基，羟基，羟基烷基，烷氧基，烷氧基烷基和烷酰基的基团。或其药学上可接受的酸加成盐。

7. 发明授权

US5631399A Process for the preparation of ethyl 3S-[[4-[[4-(aminoiminomethyl)phenyl]amino]-1,4-dioxobutyl]amino]-4-penty noate 失效
标题翻译：制备3S - [[4 - [[4-（氨基亚氨基甲基）苯基]氨基] -1,4-二氧代丁基]氨基] -4-戊酸乙酯的方法
公开(公告)号：US5631399A
公开(公告)日：1997-05-20
申请号：US647514
申请日：1996-05-14
申请人： Kevin A. Babiak , Srinivasan Babu , James R. Behling , Mark L. Boys , Kimberly J. Cain-Janicki , Wendel W. Doubleday , Payman Farid , Timothy J. Hagen , E. A. Hallinan , Donald W. Hansen, Jr. , Donald E. Korte , Kathleen T. Mc Laughlin , John R. Medich , Sean T. Nugent , Vlasdislav Orlovski , Jung M. Park , Karen B. Peterson , Daniel R. Pilipauskas , Barnett S. Pitzele , Sofya Tsymbalov , Glenn L. Stahl
发明人： Kevin A. Babiak , Srinivasan Babu , James R. Behling , Mark L. Boys , Kimberly J. Cain-Janicki , Wendel W. Doubleday , Payman Farid , Timothy J. Hagen , E. A. Hallinan , Donald W. Hansen, Jr. , Donald E. Korte , Kathleen T. Mc Laughlin , John R. Medich , Sean T. Nugent , Vlasdislav Orlovski , Jung M. Park , Karen B. Peterson , Daniel R. Pilipauskas , Barnett S. Pitzele , Sofya Tsymbalov , Glenn L. Stahl
IPC分类号： C07C227/02 , C07B61/00 , C07C227/12 , C07C227/34 , C07C229/08 , C07C257/18 , C07C229/30
CPC分类号： C07C227/12 , C07C227/34 , C07C257/18
摘要： The present invention relates to a novel process for the preparation of ethyl 3S-[[4-[[4-(aminoiminomethyl)phenyl]amino]-1,4-dioxobutyl]amino]-4-pentynoate and pharmaceutically acceptable acid addition salt thereof.
摘要翻译：本发明涉及制备3S - [[4 - [[4-（氨基亚氨基甲基）苯基]氨基] -1,4-二氧代丁基]氨基] -4-戊酸乙酯及其药学上可接受的酸加成盐的新方法。

8. 发明授权

US06344473B1 Imidazoles useful as nitric oxide synthase inhibitors 失效
标题翻译：咪唑可用作一氧化氮合酶抑制剂
公开(公告)号：US06344473B1
公开(公告)日：2002-02-05
申请号：US09633601
申请日：2000-08-07
申请人： Donald W. Hansen, Jr. , Arija A. Bergmanis , Timothy J. Hagen , E. Ann Hallinan , Steven W. Kramer , Suzanne Metz , Karen B. Peterson , Barnett S. Pitzele , Foe S. Tjoeng , Mihaly V. Toth , Mahima Trivedi , R. Keith Webber , Sofya Tsymbalov , Rolando E. Gapud
发明人： Donald W. Hansen, Jr. , Arija A. Bergmanis , Timothy J. Hagen , E. Ann Hallinan , Steven W. Kramer , Suzanne Metz , Karen B. Peterson , Barnett S. Pitzele , Foe S. Tjoeng , Mihaly V. Toth , Mahima Trivedi , R. Keith Webber , Sofya Tsymbalov , Rolando E. Gapud
IPC分类号： A61K314172
CPC分类号： C07D291/04 , C07D233/96 , C07D271/07 , C07D273/04 , C07D285/08
摘要： 1,3-diazolino and 1,3-diazolidino heterocycle derivatives useful as nitric oxide synthase inhibitors.
摘要翻译：可用作一氧化氮合酶抑制剂的1,3-二唑啉和1,3-二唑烷基杂环衍生物。

9. 发明授权

US6136829A Oxathiadiazole derivatives usful as iNOS inhibitors 失效
标题翻译： Oxathiadiazole衍生物可用作iNOS抑制剂
公开(公告)号：US6136829A
公开(公告)日：2000-10-24
申请号：US356735
申请日：1999-07-19
申请人： Donald W. Hansen, Jr. , Ariia A. Bergmanis , Timothy J. Hagen , E. Ann Hallinan , Steven W. Kramer , Suzanne Metz , Karen B. Peterson , Barnett S. Pitzele , Foe S. Tjoeng , Mihaly V. Toth , Mahima Trivedi , R. Keith Webber , Sofya Tsymbalov , Rolando E. Gapud
发明人： Donald W. Hansen, Jr. , Ariia A. Bergmanis , Timothy J. Hagen , E. Ann Hallinan , Steven W. Kramer , Suzanne Metz , Karen B. Peterson , Barnett S. Pitzele , Foe S. Tjoeng , Mihaly V. Toth , Mahima Trivedi , R. Keith Webber , Sofya Tsymbalov , Rolando E. Gapud
IPC分类号： A61K31/41 , A61K31/4166 , A61K31/4245 , A61K31/433 , A61K31/535 , A61K31/5377 , A61P9/02 , A61P43/00 , C07D233/96 , C07D271/06 , C07D271/07 , C07D273/04 , C07D285/08 , C07D291/04
CPC分类号： C07D291/04 , C07D233/96 , C07D271/07 , C07D273/04 , C07D285/08
摘要： 1,3-diazolino and 1,3-diazolidino heterocycle derivatives useful as nitric oxide synthase inhibitors.
摘要翻译：可用作一氧化氮合酶抑制剂的1,3-二唑啉和1,3-二唑烷基杂环衍生物。

10. 发明授权

US5981556A 1,3-diazolino and 1,3-diazolidino heterocycles as useful nitric oxide synthase inhibitors 失效
标题翻译： 1,3-二唑啉和1,3-二唑烷基杂环作为有用的一氧化氮合酶抑制剂
公开(公告)号：US5981556A
公开(公告)日：1999-11-09
申请号：US898110
申请日：1997-07-22
申请人： Donald W. Hansen, Jr. , Arija A. Bergmanis , Timothy J. Hagen , E. Ann Hallinan , Steven W. Kramer , Suzanne Metz , Karen B. Peterson , Barnett S. Pitzele , Foe S. Tjoeng , Mihaly V. Toth , Mahima Trivedi , R. Keith Webber , Sofya Tsymbalov , Rolando E. Gapud
发明人： Donald W. Hansen, Jr. , Arija A. Bergmanis , Timothy J. Hagen , E. Ann Hallinan , Steven W. Kramer , Suzanne Metz , Karen B. Peterson , Barnett S. Pitzele , Foe S. Tjoeng , Mihaly V. Toth , Mahima Trivedi , R. Keith Webber , Sofya Tsymbalov , Rolando E. Gapud
IPC分类号： A61K31/41 , A61K31/4166 , A61K31/4245 , A61K31/433 , A61K31/535 , A61K31/5377 , A61P9/02 , A61P43/00 , C07D233/96 , C07D271/06 , C07D271/07 , C07D273/04 , C07D285/08 , C07D291/04 , C07D285/125 , C07D417/06
CPC分类号： C07D291/04 , C07D233/96 , C07D271/07 , C07D273/04 , C07D285/08
摘要： 1,3-diazolino and 1,3-diazolidino heterocycle derivatives useful as nitric oxide synthase inhibitors.
摘要翻译：可用作一氧化氮合酶抑制剂的1,3-二唑啉和1,3-二唑烷基杂环衍生物。

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