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1. 发明授权

US07119098B2 Heteroarylakanoic acids as intergrin receptor antagonists 失效
标题翻译：杂芳基烷酸作为整合蛋白受体拮抗剂
公开(公告)号：US07119098B2
公开(公告)日：2006-10-10
申请号：US10311385
申请日：2001-06-15
申请人： Srinivasan Raj Nagarajan , Ish Kumar Khanna , Michael B. Tollefson , Scott B. Mohler , Barbara B. Chen , Mark Russell , Balekudru Devadas , Thomas D. Penning , Lori A. Schretzman , Dale P. Spangler , Mark L. Boys , Nizal S. Chandrakumar , Hwang-Fun Lu
发明人： Srinivasan Raj Nagarajan , Ish Kumar Khanna , Michael B. Tollefson , Scott B. Mohler , Barbara B. Chen , Mark Russell , Balekudru Devadas , Thomas D. Penning , Lori A. Schretzman , Dale P. Spangler , Mark L. Boys , Nizal S. Chandrakumar , Hwang-Fun Lu
IPC分类号： C07D403/12 , C07D403/14 , C07D401/12 , A61K31/443 , A61K31/4375
CPC分类号： C07D213/74 , C07D231/38 , C07D233/88 , C07D405/12 , C07D413/12 , C07D417/12 , C07D471/04
摘要： The present invention relates to a class of compounds represented by formula (I) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of Formula (I), and methods of selectively antagonizing the ανβ3 and/or the ανβ5 integrin without significantly antagonizing the IIb/IIIa integrin.
摘要翻译：本发明涉及一类由式（I）表示的化合物或其药学上可接受的盐，包含式（I）化合物的药物组合物，和选择性拮抗化合物3和/或在不显着拮抗IIb / IIIa整联蛋白的情况下，所述的5'-整联蛋白。

2. 发明授权

US06403648B2 Alkylaminoalkyl-sulfonyl-terminated &bgr;-alanineamide amino-diol compounds for treatment of hypertension 失效
标题翻译：用于治疗高血压的烷基氨基烷基 - 磺酰基封端的β-丙氨酰胺氨基二醇化合物
公开(公告)号：US06403648B2
公开(公告)日：2002-06-11
申请号：US09761907
申请日：2001-01-17
申请人： Gunnar J. Hanson , John S. Baran , Barbara B. Chen
发明人： Gunnar J. Hanson , John S. Baran , Barbara B. Chen
IPC分类号： A61K3116
CPC分类号： C07C317/44 , A61K31/16 , A61K31/165 , C07C2601/02 , C07C2601/14
摘要： Compounds characterized generally as alkylaminoalkyl-terminated &bgr;-alanineamide amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of the formula wherein n is two or three; wherein x is a number selected from zero, one and two; wherein R2 is selected from hydrido, methyl, ethyl and phenyl; wherein R3 is selected from hydrido, cyclohexylmethyl, benzyl, fluorobenzyl, chlorobenzyl, napthylmethyl, fluoronaphthylmethyl and chloronaphthylmethyl; wherein R5 is methyl; wherein R7 is cyclohexylmethyl; wherein R8 is selected from n-propyl, isobutyl, cyclopropyl, cyclopropylmethyl, allyl and vinyl; and wherein each of R9 and R10 is a group independently selected from methyl, ethyl and isopropyl; or a pharmaceutically-acceptable salt thereof.
摘要翻译：通常以烷基氨基烷基封端的β-丙氨酰胺氨基二醇衍生物表征的化合物可用作治疗高血压的肾素抑制剂。特别令人感兴趣的化合物是所述的那些，其中n是2或3; 其中x是选自零，一和二的数; 其中R2选自氢，甲基，乙基和苯基; 其中R 3选自氢，环己基甲基，苄基，氟苄基，氯苄基，萘基甲基，氟萘基甲基和氯萘基甲基; 其中R5是甲基; 其中R 7为环己基甲基; 其中R8选自正丙基，异丁基，环丙基，环丙基甲基，烯丙基和乙烯基; 并且其中R 9和R 10各自独立地选自甲基，乙基和异丙基; 或其药学上可接受的盐。

3. 发明授权

US5952381A Para-substituted phenylene derivatives 失效
标题翻译：对位取代亚苯衍生物
公开(公告)号：US5952381A
公开(公告)日：1999-09-14
申请号：US826244
申请日：1997-03-27
申请人： Barbara B. Chen , Helen Y. Chen , Glen J. Gesicki , Richard A. Haack , James W. Malecha , Thomas D. Penning , Joseph G. Rico , Thomas E. Rogers , Peter G. Ruminski , Mark A. Russell , Stella S. Yu
发明人： Barbara B. Chen , Helen Y. Chen , Glen J. Gesicki , Richard A. Haack , James W. Malecha , Thomas D. Penning , Joseph G. Rico , Thomas E. Rogers , Peter G. Ruminski , Mark A. Russell , Stella S. Yu
IPC分类号： A61K31/155 , A61K31/166 , A61K31/17 , A61K31/18 , A61K31/216 , A61K31/4168 , A61K31/4192 , A61K31/4453 , A61K31/505 , A61K31/5375 , A61P9/14 , A61P19/08 , A61P19/10 , A61P27/02 , A61P35/00 , C07C257/18 , C07C259/18 , C07C275/42 , C07C279/18 , C07C279/22 , C07C279/24 , C07C279/28 , C07C311/06 , C07C311/13 , C07C311/19 , C07C311/47 , C07C311/64 , C07C317/44 , C07C323/52 , C07D223/12 , C07D233/50 , C07D233/88 , C07D239/14 , C07D249/14 , C07D271/06 , C07D271/07 , C07D295/20 , C07D295/215 , C07D521/00 , C07C229/00 , A61K31/19 , C07C205/00
CPC分类号： C07D271/07 , A61K31/155 , C07C275/42 , C07C279/18 , C07C279/22 , C07C279/24 , C07C279/28 , C07C311/06 , C07C311/13 , C07C311/19 , C07C311/64 , C07C317/44 , C07C323/52 , C07D223/12 , C07D231/12 , C07D233/50 , C07D233/56 , C07D233/88 , C07D239/14 , C07D249/08 , C07D249/14 , C07D295/215
摘要： The present invention relates to a class of compounds represented by Formula I ##STR1## or a pharmaceutically acceptable salt thereof, pharmaceutical composition comprising compounds of the Formula I, and methods of selectively inhibiting or antagonizing the .alpha..sub.v .beta..sub.3 integrin.
摘要翻译：本发明涉及一类由式I表示的化合物或其药学上可接受的盐，包含式I化合物的药物组合物和选择性抑制或拮抗αvβ3整联蛋白的方法。

4. 发明授权

US5773646A Meta-substituted phenylene derivatives 失效
标题翻译：元取代亚苯衍生物
公开(公告)号：US5773646A
公开(公告)日：1998-06-30
申请号：US825086
申请日：1997-03-27
申请人： Nizal Chandrakumar , Barbara B. Chen , Helen Y. Chen , Michael Clare , Alan F. Gasiecki , Richard A. Haack , James W. Malecha , Peter G. Ruminski , Mark A. Russell
发明人： Nizal Chandrakumar , Barbara B. Chen , Helen Y. Chen , Michael Clare , Alan F. Gasiecki , Richard A. Haack , James W. Malecha , Peter G. Ruminski , Mark A. Russell
IPC分类号： A61K31/00 , A61K31/195 , A61K31/196 , A61K31/215 , A61K31/216 , A61K31/415 , A61K31/4164 , A61K31/4168 , A61K31/4184 , A61K31/496 , A61K31/505 , A61P1/00 , A61P1/02 , A61P19/00 , A61P19/08 , A61P19/10 , A61P27/00 , A61P27/02 , A61P35/00 , A61P43/00 , C07C45/67 , C07C49/796 , C07C205/35 , C07C205/45 , C07C205/56 , C07C205/57 , C07C257/16 , C07C257/18 , C07C259/18 , C07C275/42 , C07C279/18 , C07C279/24 , C07C279/28 , C07C311/46 , C07C311/47 , C07C317/42 , C07C317/44 , C07C323/44 , C07C323/56 , C07C335/16 , C07C335/22 , C07C335/32 , C07D223/06 , C07D233/50 , C07D233/88 , C07D235/30 , C07D239/14 , C07D311/18 , C07D311/20 , C07D405/12 , C07C241/00 , C07C205/00 , C07C229/00 , C07C321/00
CPC分类号： C07C45/673 , C07C205/35 , C07C205/45 , C07C205/56 , C07C205/57 , C07C257/16 , C07C259/18 , C07C275/42 , C07C279/18 , C07C279/24 , C07C279/28 , C07C311/46 , C07C311/47 , C07C317/42 , C07C323/44 , C07C335/16 , C07C335/22 , C07C335/32 , C07C49/796 , C07D223/06 , C07D233/50 , C07D233/88 , C07D235/30 , C07D239/14 , C07D311/18 , C07D311/20 , C07D405/12
摘要： The present invention relates to a class of compounds represented by the Formula I ##STR1## or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula I, and methods of selectively inhibiting or antagonizing the .alpha..sub.v .beta..sub.3 integrin.
摘要翻译：本发明涉及一类由式I表示的化合物或其药学上可接受的盐，包含式I化合物的药物组合物和选择性抑制或拮抗αvβ3整联蛋白的方法。

5. 发明授权

US5756549A Alkylaminoalkyl-terminated sulfide/sulfonyl-containing cycloalkyl-alanine amino-diol compounds for treatment of hypertension 失效
标题翻译：用于治疗高血压的烷基氨基烷基封端的硫化物/含磺酰基的环烷基 - 丙氨酸氨基二醇化合物
公开(公告)号：US5756549A
公开(公告)日：1998-05-26
申请号：US593026
申请日：1996-01-29
申请人： Barbara B. Chen , Gunnar J. Hanson , John S. Baran
发明人： Barbara B. Chen , Gunnar J. Hanson , John S. Baran
IPC分类号： A61K31/16 , A61K31/165 , C07C317/44 , C07C323/60
CPC分类号： C07C323/60 , A61K31/16 , A61K31/165 , C07C317/44 , C07C2101/04 , C07C2101/14 , Y10S514/912 , Y10S514/913
摘要： Compounds characterized generally as alkylaminoalkyl-terminated sulfide/sulfonyl-containing cycloalkylalkyl alanine amino-diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula II: ##STR1## wherein m is is two or three; wherein x is zero or two; wherein R.sup.2 is selected from hydrido, methyl, ethyl and phenyl; wherein R.sup.3 is selected from hydrido, cyclohexylmethyl, benzyl, fluorobenzyl, chlorobenzyl, fluoronaphthylmethyl and chloronaphthylmethyl; wherein R.sup.5 is selected from cycloalkylalkyl groups containing from three to about twelve carbon atoms; wherein R.sup.7 is cyclohexylmethyl; wherein R.sup.8 is selected from n-propyl, isobutyl, cyclopropyl;, cyclopropylmethyl, allyl and vinyl; and wherein each of R.sup.9 and R.sup.10 is a group independently selected from methyl, ethyl and isopropyl; or a pharmaceutically-acceptable salt thereof.
摘要翻译：通常作为烷基氨基烷基封端的硫化物/含磺酰基的环烷基烷基丙氨酸氨基二醇衍生物的化合物可用作治疗高血压的肾素抑制剂。特别感兴趣的化合物是式II的化合物：其中m是两个或三个; 其中x为0或2; 其中R2选自氢，甲基，乙基和苯基; 其中R 3选自氢，环己基甲基，苄基，氟苄基，氯苄基，氟萘基甲基和氯萘基甲基; 其中R 5选自含有3至约12个碳原子的环烷基烷基; 其中R 7为环己基甲基; 其中R8选自正丙基，异丁基，环丙基;环丙基甲基，烯丙基和乙烯基; 并且其中R 9和R 10各自独立地选自甲基，乙基和异丙基; 或其药学上可接受的盐。

6. 发明授权

US5432201A Alkylaminoalkyl-sulfonyl-terminated .beta.-alanineamide amino-diol compounds for treatment of hypertension 失效
标题翻译：用于治疗高血压的烷基氨基烷基 - 磺酰基封端的β-丙氨酰胺氨基二醇化合物
公开(公告)号：US5432201A
公开(公告)日：1995-07-11
申请号：US157344
申请日：1993-11-22
申请人： Gunnar J. Hanson , John S. Baran , Barbara B. Chen
发明人： Gunnar J. Hanson , John S. Baran , Barbara B. Chen
IPC分类号： A61K31/16 , A61K31/165 , C07C317/44 , C07C323/41
CPC分类号： C07C317/44 , A61K31/16 , A61K31/165 , C07C2101/02 , C07C2101/14
摘要： Compounds characterized generally as alkylaminoalkyl-terminated .beta.-alanineamide amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of the formula ##STR1## wherein n is two or three; wherein x is a number selected from zero, one and two; wherein R.sup.2 is selected from hydrido, methyl, ethyl and phenyl; wherein R.sup.3 is selected from hydrido, cyclohexylmethyl, benzyl, fluorobenzyl, chlorobenzyl, napthylmethyl, fluoronaphthylmethyl and chloronaphthylmethyl; wherein R.sup.5 is methyl; wherein R.sup.7 is cyclohexylmethyl; wherein R.sup.8 is selected from n-propyl, isobutyl, cyclopropyl, cyclopropylmethyl, allyl and vinyl; and wherein each of R.sup.9 and R.sup.10 is a group independently selected from methyl, ethyl and isopropyl; or a pharmaceutically-acceptable salt thereof.
摘要翻译：通常作为烷基氨基烷基封端的β-丙氨酸酰胺氨基二醇衍生物表征的化合物可用作治疗高血压的肾素抑制剂。特别感兴趣的化合物是下式的化合物：其中n为2或3; 其中x是选自零，一和二的数; 其中R2选自氢，甲基，乙基和苯基; 其中R 3选自氢，环己基甲基，苄基，氟苄基，氯苄基，萘基甲基，氟萘基甲基和氯萘基甲基; 其中R5是甲基; 其中R 7为环己基甲基; 其中R8选自正丙基，异丁基，环丙基，环丙基甲基，烯丙基和乙烯基; 并且其中R 9和R 10各自独立地选自甲基，乙基和异丙基; 或其药学上可接受的盐。

7. 发明授权

US5312838A .beta.-alanineamide aryl/alkylsulfide/sulfonyl-terminated amino-diol compounds for treatment of hypertension 失效
标题翻译：用于治疗高血压的β-丙氨酸酰胺芳基/烷基硫化物/磺酰基封端的氨基二醇化合物
公开(公告)号：US5312838A
公开(公告)日：1994-05-17
申请号：US949194
申请日：1992-09-21
申请人： Barbara B. Chen , Gunnar J. Hanson , John S. Baran
发明人： Barbara B. Chen , Gunnar J. Hanson , John S. Baran
IPC分类号： C07C317/44 , C07C323/60 , A61K31/16 , A61K31/165 , C07C317/50 , C07C323/41
CPC分类号： C07C317/44 , C07C323/60 , C07C2101/14
摘要： Compounds characterized generally as .beta.-alanineamide aryl/alkylsulfide/sulfonyl-terminated amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of the formula ##STR1## wherein R.sup.1 is selected from isopropyl, isobutyl, sec-butyl, tert-butyl, phenyl, fluorophenyl, chlorophenyl, benzyl, fluorobenzyl, chlorobenzyl, naphthyl, fluoronaphthyl, chloronaphthyl, fluoronaphthylmethyl and chloronaphthylmethyl; wherein x is zero or two; wherein R.sup.2 is selected from hydrido, methyl, ethyl and phenyl; wherein R.sup.3 is selected from hydrido, cyclohexylmethyl, benzyl, fluorobenzyl, chlorobenzyl, fluoronaphthylmethyl and chloronaphthylmethyl; wherein R.sup.5 is selected from methyl and ethyl; wherein R.sup.7 is cyclohexylmethyl; and wherein R.sup.8 is selected from n-propyl, isobutyl, cyclopropyl, cyclopropylmethyl, allyl and vinyl.
摘要翻译：通常以β-丙氨酰胺芳基/烷基硫醚/磺酰基封端的氨基二醇衍生物为特征的化合物可用作治疗高血压的肾素抑制剂。特别感兴趣的化合物是下式的化合物，其中R 1选自异丙基，异丁基，仲丁基，叔丁基，苯基，氟苯基，氯苯基，苄基，氟苄基，氯苄基，萘基，氟萘基，氯萘基，氟萘基甲基和氯萘基甲基 ; 其中x为0或2; 其中R2选自氢，甲基，乙基和苯基; 其中R 3选自氢，环己基甲基，苄基，氟苄基，氯苄基，氟萘基甲基和氯萘基甲基; 其中R 5选自甲基和乙基; 其中R 7为环己基甲基; 并且其中R8选自正丙基，异丁基，环丙基，环丙基甲基，烯丙基和乙烯基。

8. 发明授权

US07115596B2 Thiazole compounds as integrin receptor antagonists derivatives 失效
标题翻译：噻唑化合物作为整合素受体拮抗剂衍生物
公开(公告)号：US07115596B2
公开(公告)日：2006-10-03
申请号：US10741056
申请日：2003-12-19
申请人： John A. Wendt , Heather Stenmark , Hongwei Wu , Yaping Wang , Barbara B. Chen , Thomas D. Penning , Victoria L. Downs , Mark L. Boys , Mark Russell , Dale P. Spangler
发明人： John A. Wendt , Heather Stenmark , Hongwei Wu , Yaping Wang , Barbara B. Chen , Thomas D. Penning , Victoria L. Downs , Mark L. Boys , Mark Russell , Dale P. Spangler
IPC分类号： A61K31/55 , A61K31/5025 , A61K31/44 , A61K31/425 , A61K31/36 , C07D401/00 , C07D417/00 , C07D413/00 , C07D471/02 , C07D207/00 , C07D317/46
CPC分类号： C07D417/14 , C07D471/04
摘要： The present invention relates to a class of compounds represented by the Formula I or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula I, and methods of selectively inhibiting or antagonizing the αvβ3 and/or the αvβ5 integrin without significantly inhibiting the αvβ6 integrin.
摘要翻译：本发明涉及一类由式I表示的化合物或其药学上可接受的盐，包含式I化合物的药物组合物和选择性抑制或拮抗α > 3和/或α5β5整联蛋白，而不显着抑制α3β6 整合素。

9. 发明授权

US06531494B1 Gem-substituted &agr;v&bgr;3 antagonists 失效
标题翻译：宝石取代的alphavbeta3拮抗剂
公开(公告)号：US06531494B1
公开(公告)日：2003-03-11
申请号：US09942214
申请日：2001-08-29
申请人： Ish Kumar Khanna , Yi Yu , Balekudru Devadas , Hwang-Fun Lu , Nizal S Chandrakumar , Renee M. Huff , Bipinchandra N. Desai , Srinivasan Raj Nagarajan , Alan F. Gasiecki , Thomas D. Penning , Mark A. Russell , Mark L. Boys , Lori A. Schretzman , Barbara B. Chen , Thomas Rogers , John Adam Wendt , Albert Khilevich , Yaping Wang
发明人： Ish Kumar Khanna , Yi Yu , Balekudru Devadas , Hwang-Fun Lu , Nizal S Chandrakumar , Renee M. Huff , Bipinchandra N. Desai , Srinivasan Raj Nagarajan , Alan F. Gasiecki , Thomas D. Penning , Mark A. Russell , Mark L. Boys , Lori A. Schretzman , Barbara B. Chen , Thomas Rogers , John Adam Wendt , Albert Khilevich , Yaping Wang
IPC分类号： A61K3144
CPC分类号： C07D213/74 , C07D213/73 , C07D401/12 , C07D471/04
摘要： The present invention relates to a class of compounds represented by the Formula I. or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula I, and methods of selectively inhibiting or antagonizing the &agr;V&bgr;3 and/or the &agr;V&bgr;5 integrin.
摘要翻译：本发明涉及一类由式I表示的化合物或其药学上可接受的盐，包含式I化合物的药物组合物，以及选择性抑制或拮抗αVβ3和/或αVβ5整联蛋白的方法。

10. 发明授权

US5773644A Cyclopropyl alkanoic acid derivatives 失效
标题翻译：环丙基链烷酸衍生物
公开(公告)号：US5773644A
公开(公告)日：1998-06-30
申请号：US825040
申请日：1997-03-27
申请人： Barbara B. Chen , Helen Y. Chen , Michael Clare , Shashidhar N. Rao , Mark A. Russell
发明人： Barbara B. Chen , Helen Y. Chen , Michael Clare , Shashidhar N. Rao , Mark A. Russell
IPC分类号： C07D239/14 , A61K31/00 , A61K31/195 , A61K31/196 , A61K31/215 , A61K31/216 , A61K31/505 , A61P3/00 , A61P3/14 , A61P9/00 , A61P9/10 , A61P35/00 , A61P35/04 , A61P43/00 , C07C279/18 , C07C279/24 , C07D239/42 , C07C241/00 , C07C229/00 , C07D239/00
CPC分类号： C07D239/42 , C07C279/18 , C07C279/24 , C07C2101/02
摘要： The present invention relates to a class of compounds represented by the Formula I ##STR1## or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula I, and methods of selectively inhibiting or antagonizing the .alpha..sub.v .beta..sub.3 integrin.
摘要翻译：本发明涉及一类由式I表示的化合物或其药学上可接受的盐，包含式I化合物的药物组合物和选择性抑制或拮抗αvβ3整联蛋白的方法。

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