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1. 发明申请

US20130281385A1 SMALL MOLECULE APOPTOSIS PROMOTERS 失效
标题翻译：小分子疫苗促进剂
公开(公告)号：US20130281385A1
公开(公告)日：2013-10-24
申请号：US13536974
申请日：2012-06-28
申请人： Gunnar J. Hanson , Davis Thomas , Nizal Chandrakumar , Susan Harran
发明人： Gunnar J. Hanson , Davis Thomas , Nizal Chandrakumar , Susan Harran
IPC分类号： A61K38/06 , C07K5/02
CPC分类号： C07D207/16 , C07D249/04 , C07D403/06 , C07D403/10 , C07D403/14 , C07D487/14
摘要： The invention provides small molecule mimics of the Smac peptide that are dimer- or dimer-like compounds having two amide-containing domains connected by a linker. These compounds are useful to promote apoptosis. The invention includes pharmaceutical compositions comprising such compounds and methods to use them to treat conditions including cancer and autoimmune disorders.
摘要翻译：本发明提供Smac肽的小分子模拟物，其是具有通过接头连接的两个含酰胺的结构域的二聚体或二聚体样化合物。这些化合物可用于促进凋亡。本发明包括包含这些化合物的药物组合物和使用它们来治疗包括癌症和自身免疫疾病的病症的方法。

2. 发明授权

US08222291B2 Small molecule apoptosis promoters 失效
公开(公告)号：US08222291B2
公开(公告)日：2012-07-17
申请号：US12897760
申请日：2010-10-04
申请人： Gunnar J. Hanson , David Thomas , Nizal Chandrakumar , Susan Harran
发明人： Gunnar J. Hanson , David Thomas , Nizal Chandrakumar , Susan Harran
IPC分类号： A61K31/40 , C07D207/04
CPC分类号： C07D207/16 , C07D249/04 , C07D403/06 , C07D403/10 , C07D403/14 , C07D487/14
摘要： The invention provides small molecule mimics of the Smac peptide that are dimer- or dimer-like compounds having two amide-containing domains connected by a linker. These compounds are useful to promote apoptosis. The invention includes pharmaceutical compositions comprising such compounds and methods to use them to treat conditions including cancer and autoimmune disorders.

3. 发明授权

US08586542B2 Small molecule apoptosis promoters 失效
标题翻译：小分子凋亡启动子
公开(公告)号：US08586542B2
公开(公告)日：2013-11-19
申请号：US13536974
申请日：2012-06-28
申请人： Gunnar J. Hanson , David Thomas , Nizal Chandrakumar , Susan Harran
发明人： Gunnar J. Hanson , David Thomas , Nizal Chandrakumar , Susan Harran
IPC分类号： A61K38/00
CPC分类号： C07D207/16 , C07D249/04 , C07D403/06 , C07D403/10 , C07D403/14 , C07D487/14
摘要： The invention provides small molecule mimics of the Smac peptide that are dimer- or dimer-like compounds having two amide-containing domains connected by a linker. These compounds are useful to promote apoptosis. The invention includes pharmaceutical compositions comprising such compounds and methods to use them to treat conditions including cancer and autoimmune disorders.
摘要翻译：本发明提供Smac肽的小分子模拟物，其是具有通过接头连接的两个含酰胺的结构域的二聚体或二聚体样化合物。这些化合物可用于促进凋亡。本发明包括包含这些化合物的药物组合物和使用它们来治疗包括癌症和自身免疫疾病的病症的方法。

4. 发明授权

US07807699B2 Dimeric pyrrolidine amide-containing small molecule apoptosis promoters 有权
标题翻译：含二聚吡咯烷酰胺的小分子凋亡启动子
公开(公告)号：US07807699B2
公开(公告)日：2010-10-05
申请号：US11726602
申请日：2007-03-21
申请人： Gunnar J. Hanson , David Thomas , Nizal Chandrakumar , Susan Harran
发明人： Gunnar J. Hanson , David Thomas , Nizal Chandrakumar , Susan Harran
IPC分类号： A01N43/64
CPC分类号： C07D207/16 , C07D249/04 , C07D403/06 , C07D403/10 , C07D403/14 , C07D487/14
摘要： The invention provides small molecule mimics of the Smac peptide that are dimer- or dimer-like compounds having two amide-containing domains connected by a linker. These compounds are useful to promote apoptosis. The invention includes pharmaceutical compositions comprising such compounds and methods to use them to treat conditions including cancer and autoimmune disorders.
摘要翻译：本发明提供Smac肽的小分子模拟物，其是具有通过接头连接的两个含酰胺的结构域的二聚体或二聚体样化合物。这些化合物可用于促进凋亡。本发明包括包含这些化合物的药物组合物和使用它们来治疗包括癌症和自身免疫疾病的病症的方法。

5. 发明申请

US20120082640A1 Small molecule apoptosis promoters 失效
标题翻译：小分子凋亡启动子
公开(公告)号：US20120082640A1
公开(公告)日：2012-04-05
申请号：US12897760
申请日：2010-10-04
申请人： Gunnar J. Hanson , David Thomas , Nizal Chandrakumar , Susan Harran
发明人： Gunnar J. Hanson , David Thomas , Nizal Chandrakumar , Susan Harran
IPC分类号： A61K31/40 , A61K31/551 , A61K31/4192 , A61P37/00 , C07D487/14 , A61K31/4985 , A61P35/04 , C07D401/12 , C07D249/04
CPC分类号： C07D207/16 , C07D249/04 , C07D403/06 , C07D403/10 , C07D403/14 , C07D487/14
摘要： The invention provides small molecule mimics of the Smac peptide that are dimer- or dimer-like compounds having two amide-containing domains connected by a linker. These compounds are useful to promote apoptosis. The invention includes pharmaceutical compositions comprising such compounds and methods to use them to treat conditions including cancer and autoimmune disorders.
摘要翻译：本发明提供Smac肽的小分子模拟物，其是具有通过接头连接的两个含酰胺的结构域的二聚体或二聚体样化合物。这些化合物可用于促进凋亡。本发明包括包含这些化合物的药物组合物和使用它们来治疗包括癌症和自身免疫疾病的病症的方法。

6. 发明授权

US06777572B2 Use of propargyl glycine amino propargyl diol compounds for treatment of renal failure 失效
标题翻译：使用炔丙基甘氨酸氨基炔丙醇二醇化合物治疗肾衰竭
公开(公告)号：US06777572B2
公开(公告)日：2004-08-17
申请号：US09996345
申请日：2001-11-28
申请人： Gunnar J. Hanson , John S. Baran
发明人： Gunnar J. Hanson , John S. Baran
IPC分类号： C07C30300
CPC分类号： C07C237/22 , C07C271/20 , C07C2601/14 , C07D277/30
摘要： Compounds characterized generally as propargyl glycine amino propargyl diol derivatives are useful for treatment of renal failure. Compounds of particular interest are those of Formula I wherein A is selected from CO and SO2 wherein X is selected from oxygen atom and methylene; wherein each of R1 and R9 is a group independently selected from hydrido, methyl, ethyl, n-propyl, isopropyl, benzyl, b, b, b-trifluoroethyl, t-butyloxycarbonyl and methoxymethylcarbonyl, and wherein the nitrogen atom to which R1 and R9 are attached may be combined with oxygen to form an N-oxide; wherein R2 is selected from hydrido, methyl, ethyl and isopropyl; wherein R3 is selected from benzyl, cyclohexylmethyl, phenethyl, imidazolemethyl, pyridylmethyl and 2-pyridylethyl; wherein each of R5 and R8 is independently propargyl or a propargyl-containing moiety; wherein R7 is cyclohexylmethyl; wherein each of R4 and R6 is independently selected from hydrido and methyl; wherein each of R11 and R12 is independently selected from hydrido, alkyl and phenyl; wherein m is zero; and wherein n is a number selected from zero through three; or a pharmaceutically-acceptable salt thereof.
摘要翻译：通常被称为炔丙基甘氨酸氨基炔丙醇二醇衍生物的化合物可用于治疗肾功能衰竭。特别感兴趣的化合物是式I的化合物，其中A选自CO和SO 2，其中X选自氧原子和亚甲基; 其中R 1和R 9各自独立地选自氢，甲基，乙基，正丙基，异丙基，苄基，b，b，b-三氟乙基，叔丁氧基羰基和甲氧基甲基羰基，其中R1和R9 可以与氧结合形成N-氧化物; 其中R2选自氢，甲基，乙基和异丙基; 其中R 3选自苄基，环己基甲基，苯乙基，咪唑甲基，吡啶基甲基和2-吡啶基乙基; 其中R 5和R 8各自独立地是炔丙基或含炔丙基的部分; 其中R 7为环己基甲基; 其中R 4和R 6各自独立地选自氢和甲基; 其中R 11和R 12各自独立地选自氢，烷基和苯基; 其中m为零; 并且其中n是选自0至3的数字; 或其药学上可接受的盐。

7. 发明授权

US06667414B2 Use of propargyl glycine amino propargyl diol compounds for treatment of congestive heart failure 失效
标题翻译：使用炔丙基甘氨酸氨基炔丙基二醇化合物治疗充血性心力衰竭
公开(公告)号：US06667414B2
公开(公告)日：2003-12-23
申请号：US09996344
申请日：2001-11-28
申请人： Gunnar J. Hanson , John S. Baran
发明人： Gunnar J. Hanson , John S. Baran
IPC分类号： C07C30300
CPC分类号： C07C237/22 , C07C271/20 , C07C2601/14 , C07D277/30
摘要： Compounds characterized generally as propargyl glycine amino propargyl diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula I wherein A is selected from CO and SO2 wherein X is selected from oxygen atom and methylene; wherein each of R1 and R9 is a group independently selected from hydrido, methyl, ethyl, n-propyl, isopropyl, benzyl, b, b, b-trifluoroethyl, t-butyloxycarbonyl and methoxymethylcarbonyl, and wherein the nitrogen atom to which R1 and R9 are attached may be combined with oxygen to form an N-oxide; wherein R2 is selected from hydrido, methyl, ethyl and isopropyl; wherein R3 is selected from benzyl, cyclohexylmethyl, phenethyl, imidazolemethyl, pyridylmethyl and 2-pyridylethyl; wherein each of R5 and R8 is independently propargyl or a propargyl-containing moiety; wherein R7 is cyclohexylmethyl; wherein each of R4 and R6 is independently selected from hydrido and methyl; wherein each of R11 and R12 is independently selected from hydrido, alkyl and phenyl; wherein m is zero; and wherein n is a number selected from zero through three; or a pharmaceutically-acceptable salt thereof.
摘要翻译：通常作为炔丙基甘氨酸氨基炔丙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式I的化合物，其中A选自CO和SO 2，其中X选自氧原子和亚甲基; 其中R 1和R 9各自独立地选自氢，甲基，乙基，正丙基，异丙基，苄基，b，b，b-三氟乙基，叔丁氧基羰基和甲氧基甲基羰基，其中R1和R9 可以与氧结合形成N-氧化物; 其中R2选自氢，甲基，乙基和异丙基; 其中R 3选自苄基，环己基甲基，苯乙基，咪唑甲基，吡啶基甲基和2-吡啶基乙基; 其中R 5和R 8各自独立地是炔丙基或含炔丙基的部分; 其中R 7为环己基甲基; 其中R 4和R 6各自独立地选自氢和甲基; 其中R 11和R 12各自独立地选自氢，烷基和苯基; 其中m为零; 并且其中n是选自0至3的数字; 或其药学上可接受的盐。

8. 发明授权

US06617324B1 Substituted pyrazoles as p38 kinase inhibitors 失效
标题翻译：取代的吡唑作为p38激酶抑制剂
公开(公告)号：US06617324B1
公开(公告)日：2003-09-09
申请号：US10114297
申请日：2002-04-02
申请人： Ashok S. Naraian , Michael Clare , Paul W. Collins , Joyce Zuowu Crich , Rajesh Devraj , Daniel L. Flynn , Lifeng Geng , Matthew J. Graneto , Cathleen E. Hanau , Gunnar J. Hanson , Susan J. Hartmann , Michael Hepperle , He Huang , Francis J. Koszyk , Shuyuan Liao , Suzanne Metz , Richard A. Partis , Thao D. Perry , Shashidhar N. Rao , Shaun Raj Selness , Michael S. South , Michael A. Stealey , John Jeffrey Talley , Michael L. Vazquez , Richard M. Weier , Xiangdong Xi , Ish K. Khanna , Yi Yu
发明人： Ashok S. Naraian , Michael Clare , Paul W. Collins , Joyce Zuowu Crich , Rajesh Devraj , Daniel L. Flynn , Lifeng Geng , Matthew J. Graneto , Cathleen E. Hanau , Gunnar J. Hanson , Susan J. Hartmann , Michael Hepperle , He Huang , Francis J. Koszyk , Shuyuan Liao , Suzanne Metz , Richard A. Partis , Thao D. Perry , Shashidhar N. Rao , Shaun Raj Selness , Michael S. South , Michael A. Stealey , John Jeffrey Talley , Michael L. Vazquez , Richard M. Weier , Xiangdong Xi , Ish K. Khanna , Yi Yu
IPC分类号： A61K31496
CPC分类号： C07D409/14 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/14 , C07D413/14 , C07D417/14 , C07D453/02 , C07D471/04 , C07D473/00 , C07D487/04
摘要： A class of pyrazole derivatives described for use in treating p38 kinase mediated disorders. Compounds of particular interest are defined by Formula IA wherein R1, R2, R3 and R4 are as described in the specification.
摘要翻译：一类描述用于治疗p38激酶介导的病症的吡唑衍生物。特别感兴趣的化合物由式IA定义，其中R1，R2，R3和R4如说明书中所述。

9. 发明授权

US06174923B1 Use of ethynyl alanine amino diol compounds for treatment of renin-mediated disorders 失效
标题翻译：乙炔丙氨酸二氨基二醇化合物用于治疗肾素介导的疾病
公开(公告)号：US06174923B1
公开(公告)日：2001-01-16
申请号：US09239493
申请日：1999-01-28
申请人： Gunnar J. Hanson , John S. Baran
发明人： Gunnar J. Hanson , John S. Baran
IPC分类号： A61K31165
CPC分类号： A61K31/18 , A61K31/165 , C07C237/22 , C07C271/20 , C07C311/13 , C07C2601/02 , C07C2601/14
摘要： Compounds characterized generally as ethynyl alanine amino diol derivatives are useful to treat disorders mediated by plasma renin activity. Compounds of particular interest are renin inhibitors of Formula I wherein A is selected from CO and SO2 wherein X is selected from oxygen atom and methylene; wherein each of R1 and R9 is a group independently selected from hydrido, methyl, ethyl, n-propyl, isopropyl, benzyl, &bgr;,&bgr;,&bgr;-trifluoroethyl, t-butyloxycarbonyl and methoxymethylcarbonyl, and wherein the nitrogen atom to which R1 and R9 are attached may be combined with oxygen to form an N-oxide; wherein R2 is selected from hydrido, methyl, ethyl and isopropyl; wherein R3 is selected from benzyl, cyclohexylmethyl, phenethyl, imidazolemethyl, pyridylmethyl and 2-pyridylethyl; wherein R5 is propargyl or a propargyl-containing moiety; wherein R7 is cyclohexylmethyl; wherein each of R4 and R6 is independently selected from hydrido and methyl; wherein R8 is selected from ethyl, n-propyl, isobutyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cyclopropylmethyl, cyclohexylmethyl, cyclohexylethyl, allyl, vinyl and fluorovinyl; wherein each of R11 and R12 is independently selected from hydrido, alkyl and phenyl; wherein m is zero; and wherein n is a number selected from zero through three; or a pharmaceutically-acceptable salt thereof.
摘要翻译：通常被称为乙炔基丙氨酸氨基二醇衍生物的化合物可用于治疗由血浆肾素活性介导的病症。特别感兴趣的化合物是式I的肾素抑制剂，其中A选自CO和SO 2，其中X选自氧原子和亚甲基; 其中R 1和R 9各自独立地选自氢，甲基，乙基，正丙基，异丙基，苄基，β，β，β-三氟乙基，叔丁氧基羰基和甲氧基甲基羰基，其中R1和R9 可以与氧结合形成N-氧化物; 其中R2选自氢，甲基，乙基和异丙基; 其中R 3选自苄基，环己基甲基，苯乙基，咪唑甲基，吡啶基甲基和2-吡啶基乙基; 其中R5是炔丙基或含炔丙基的部分; 其中R 7为环己基甲基; 其中R 4和R 6各自独立地选自氢和甲基; 其中R8选自乙基，正丙基，异丁基，环丙基，环丁基，环戊基，环己基，环丙基甲基，环己基甲基，环己基乙基，烯丙基，乙烯基和氟乙烯基; 其中R 11和R 12各自独立地选自氢，烷基和苯基; 其中m为零; 并且其中n是选自0至3的数字; 或其药学上可接受的盐。

10. 发明授权

US6087496A Substituted pyrazoles suitable as p38 kinase inhibitors 失效
标题翻译：适合作为p38激酶抑制剂的取代的吡唑
公开(公告)号：US6087496A
公开(公告)日：2000-07-11
申请号：US283718
申请日：1999-04-01
申请人： Ashok Anantanarayan , Michael Clare , Lifeng Geng , Gunnar J. Hanson , Richard A. Partis , Michael A. Stealey , Richard M. Weier
发明人： Ashok Anantanarayan , Michael Clare , Lifeng Geng , Gunnar J. Hanson , Richard A. Partis , Michael A. Stealey , Richard M. Weier
IPC分类号： A61K31/44 , A61K31/445 , A61K31/5377 , C07D401/04 , C07D401/14 , C07D403/04 , C07D413/04
CPC分类号： C07D401/04 , C07D401/14
摘要： A class of pyrazole derivatives is described for use in treating p38 kinase mediated disorders. Compounds of particular interest are defined by Formula I: ##STR1## wherein R.sup.1, R.sup.2, Ar.sup.1 and HetAr.sup.2 are as described in the specification.
摘要翻译：描述了一类吡唑衍生物用于治疗p38激酶介导的病症。特别感兴趣的化合物由式I定义：其中R1，R2，Ar1和HetAr2如说明书中所述。

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