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1. 发明申请

US20150018328A1 THERAPEUTICALLY ACTIVE COMPOUNDS AND THEIR METHODS OF USE 有权
标题翻译：治疗活性化合物及其使用方法
公开(公告)号：US20150018328A1
公开(公告)日：2015-01-15
申请号：US14328885
申请日：2014-07-11
申请人： Zenon D. Konteatis , Janeta Popovici-Muller , Jeremy Travins , Robert Zahler , Zhenwei Cai , Ding Zhou
发明人： Zenon D. Konteatis , Janeta Popovici-Muller , Jeremy Travins , Robert Zahler , Zhenwei Cai , Ding Zhou
IPC分类号： C07D417/04 , A61K31/53 , A61K45/06 , C07D251/18 , C07D413/04 , C07D405/14 , C07D405/12 , C07D403/04 , A61K31/5377 , C07D401/04 , C07D401/14
CPC分类号： A61K31/53 , A61K31/506 , A61K31/5377 , A61K45/06 , C07D251/18 , C07D251/48 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/10 , C07D405/12 , C07D405/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14
摘要： Provided are compounds useful for treating cancer and methods of treating cancer comprising administering to a subject in need thereof a compound described herein.
摘要翻译：提供的是用于治疗癌症的化合物和治疗癌症的方法，包括向有需要的受试者施用本文所述的化合物。

2. 发明授权

US07687495B2 Substituted piperidines 失效
标题翻译：取代的哌啶
公开(公告)号：US07687495B2
公开(公告)日：2010-03-30
申请号：US12076221
申请日：2008-03-14
申请人： Peter Herold , Robert Mah , Vincenzo Tschinke , Christiane Marti , Stefan Stutz , Stjepan Jelakovic , Zenon D. Konteatis , Jennifer L. Ludington , Michael Quirmbach , Aleksandar Stojanovic , Dirk Behnke , Frank Hollinger
发明人： Peter Herold , Robert Mah , Vincenzo Tschinke , Christiane Marti , Stefan Stutz , Stjepan Jelakovic , Zenon D. Konteatis , Jennifer L. Ludington , Michael Quirmbach , Aleksandar Stojanovic , Dirk Behnke , Frank Hollinger
IPC分类号： C07D401/02 , A61K31/50 , A61K31/4965
CPC分类号： C07D413/12 , C07D413/14
摘要： Substituted piperidines of formulae (I) and (II) with the substituent definitions as explained in the specification. The compounds are suitable in particular as renin inhibitors and are highly potent.
摘要翻译：式（I）和（II）的取代的哌啶与说明书中所述的取代基定义相同。该化合物特别适合作为肾素抑制剂，并且是非常有效的。

3. 发明授权

US07741479B2 Urea inhibitors of MAP kinases 失效
标题翻译： MAP激酶的尿素抑制剂
公开(公告)号：US07741479B2
公开(公告)日：2010-06-22
申请号：US11295638
申请日：2005-12-07
申请人： Enrique Luis Michelotti , Eric Bruce Springman , Duyan Nguyen , Rupa S. Shetty , Younghee Lee , Kristofer Kent Moffett , Jennifer Lee Ludington , Ted Tsutomis Fujimoto , Zenon D. Konteatis , Bin Liu , Frank Hollinger , Bruce D. Dorsey
发明人： Enrique Luis Michelotti , Eric Bruce Springman , Duyan Nguyen , Rupa S. Shetty , Younghee Lee , Kristofer Kent Moffett , Jennifer Lee Ludington , Ted Tsutomis Fujimoto , Zenon D. Konteatis , Bin Liu , Frank Hollinger , Bruce D. Dorsey
IPC分类号： C07D273/06
CPC分类号： C07D333/38 , C07D231/40 , C07D243/08 , C07D277/48 , C07D277/56 , C07D295/192 , C07D333/36 , C07D403/06 , C07D405/06 , C07D409/04 , C07D409/06 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/06 , C07D417/14 , C07D495/04
摘要： The present invention is directed to a compound having the formula wherein R1, R2, G, and Q are defined herein. The compounds of the present invention are useful as inhibitors of protein kinases such as MAP kinases, in particular p38 kinases. The present invention is also directed to compositions comprising a compound according to the above formula. The compounds and compositions described herein are useful for treating and preventing an inflammatory condition or disease. The present invention is also directed to a method of treating or preventing a protein kinase-mediated condition.
摘要翻译：本发明涉及具有下式的化合物：其中R1，R2，G和Q如本文所定义。本发明的化合物可用作蛋白激酶如MAP激酶，特别是p38激酶的抑制剂。本发明还涉及包含根据上式的化合物的组合物。本文所述的化合物和组合物可用于治疗和预防炎性疾病或疾病。本发明还涉及治疗或预防蛋白激酶介导的病症的方法。

4. 发明申请

US20080171748A1 Substituted piperidines 失效
标题翻译：取代的哌啶
公开(公告)号：US20080171748A1
公开(公告)日：2008-07-17
申请号：US12076221
申请日：2008-03-14
申请人： Peter Herold , Robert Mah , Vincenzo Tschinke , Christiane Marti , Stefan Stutz , Stjepan Jelakovic , Zenon D. Konteatis , Jennifer L. Ludington , Michael Quirmbach , Aleksandar Stojanovic , Dirk Behnke , Frank Hollinger
发明人： Peter Herold , Robert Mah , Vincenzo Tschinke , Christiane Marti , Stefan Stutz , Stjepan Jelakovic , Zenon D. Konteatis , Jennifer L. Ludington , Michael Quirmbach , Aleksandar Stojanovic , Dirk Behnke , Frank Hollinger
IPC分类号： A61K31/50 , A61K31/4965
CPC分类号： C07D413/12 , C07D413/14
摘要： Substituted piperidines of formulae (I) and (II) with the substituent definitions as explained in the specification. The compounds are suitable in particular as renin inhibitors and are highly potent.
摘要翻译：式（I）和（II）的取代的哌啶与说明书中所述的取代基定义相同。该化合物特别适合作为肾素抑制剂，并且是非常有效的。

5. 发明授权

US5494898A Peptide skeletal muscle relaxants 失效
标题翻译：肽骨骼肌松弛剂
公开(公告)号：US5494898A
公开(公告)日：1996-02-27
申请号：US303975
申请日：1994-09-09
申请人： Yea-Shun Cheng , Zenon D. Konteatis , Mark J. Macielag , David C. Palmer
发明人： Yea-Shun Cheng , Zenon D. Konteatis , Mark J. Macielag , David C. Palmer
IPC分类号： A61K38/00 , C07K5/02 , C07K5/087 , C07K5/09 , C07K5/097 , A61K38/06
CPC分类号： C07K5/0821 , C07K5/0202 , C07K5/0812 , C07K5/0815 , C07K5/0823 , A61K38/00
摘要： Novel diquaternary polypeptides possessing skeletal muscle relaxation activity represented by the formulae: ##STR1## wherein: R is lower alkyl; R.sub.1 and R.sub.2 are lower alkyl or R.sub.1 and R.sub.2, together with the nitrogen to which they are attached form a heterocyclic ring having 5 to 7 member atoms; R.sub.3 is lower alkyl, [N,N-di(lower alkyl)-3-piperidinium].sup.(+), or [N,N-di(lower alkyl)-4-piperidinium].sup.(+) R.sub.4 is selected from the group consisting of t-butyl, benzyl or fluorenylmethyl; A.sub.1 is selected from the group consisting of trans-4-acetoxyproline, phenylalanine, glutamic acid-.gamma.-methyl ester, or proline; AA.sub.2 is selected from the group consisting of phenylalanine, leucine, 3-(2-naphthyl)alanine, 3-(1-naphthyl)alanine, and 3-cyclohexylalanine; AA.sub.3 is proline when R.sub.3 is [N,N-di(lower alkyl)-3-piperidinium].sup.(+) or [N,N-di(lower alkyl)-4-piperidinium].sup.(+), and is Orn(.delta.-N.sup.(+) --R--R.sub.1 --R.sub.2) or Lys(.epsilon.-N.sup.(+) --R--R.sub.1 --R.sub.2) when R.sub.3 ia lower alkyl; AA.sub.4 is Orn(.delta.-N.sup.(+)--R--R.sub.1 --R.sub.2) or Lys(.epsilon.-N.sup.(+) --R--R.sub.1 --R.sub.2); Z.sup.(-) is a pharmaceutically acceptable anion; and (R).sub.m R.sub.1 R.sub.2 N.sup.(+) represents the acceptable anion; (R).sub.m R.sub.1 R.sub.2 N.sup.(+) -- represents the alpha amino group of AA.sub.1 ; and m represents an integer of 0 or 1 with the proviso that m is zero only when AA.sub.1 is trans-4-acetoxyproline or proline.
摘要翻译：具有由下式表示的骨骼肌松弛活性的新型二季铵化多肽：其中：R为低级烷基; R 1和R 2是低级烷基或R 1和R 2与它们所连接的氮一起形成具有5至7个成员原子的杂环; R3是低级烷基，[N，N-二（低级烷基）-3-哌啶鎓]（+）或[N，N-二（低级烷基）-4-哌啶鎓]（+）R 4选自叔丁基，苄基或芴基甲基; A1选自反式-4-乙酰氧基脯氨酸，苯丙氨酸，谷氨酸-γ-甲酯或脯氨酸; AA2选自苯丙氨酸，亮氨酸，3-（2-萘基）丙氨酸，3-（1-萘基）丙氨酸和3-环己基丙氨酸; 当R3是[N，N-二（低级烷基）-3-哌啶鎓]（+）或[N，N-二（低级烷基）-4-哌啶鎓]（+）时，AA3是脯氨酸，并且是Orn 当R3低级烷基时，N（+） - R-R1-R2）或Lys（ε-N（+） - R-R1-R2） AA4是Orn（Δ-N（+）-R-R1-R2）或Lys（ε-N（+）-R-R1-R2）; Z（ - ）是药学上可接受的阴离子; 和（R）mR1R2N（+）表示可接受的阴离子; （R）mR1R2N（+） - 表示AA1的α氨基; m表示0或1的整数，条件是仅当AA1为反式-4-乙酰氧基脯氨酸或脯氨酸时，m为0。

6. 发明授权

US5190924A Peptide amides and amide dimers useful as muscle relaxants 失效
标题翻译：肽类辅助剂和辅助剂可用作肌肉松弛剂
公开(公告)号：US5190924A
公开(公告)日：1993-03-02
申请号：US654736
申请日：1991-02-13
申请人： Zenon D. Konteatis , David C. Palmer
发明人： Zenon D. Konteatis , David C. Palmer
IPC分类号： A61K31/16 , A61K38/00 , A61P21/02 , C07C237/22 , C07K5/06 , C07K5/065 , C07K5/08 , C07K5/087 , C07K5/10
CPC分类号： C07K5/0812 , C07K5/06078 , Y10S514/906
摘要： Peptide amide and amide dimer muscle relaxants represented by the formulae: ##STR1## wherein: R is lower alkyl; R.sub.1 and R.sub.2 independently selected from the group consisting of hydrogen, lower alkyl, allyl, propargyl, aryl lower alkyl and cyclo-lower alkyl lower alkyl, or R plus one or both of R.sub.1 and R.sub.2, together with the nitrogen to which they are attached, form a heterocyclic ring having 5 to 7 member atoms; AA are independently selected from certain amino acids moieties; n is 2 to 4; x is independently 0 or 1; y is independently 1 or 2; z is 2 to 12; and An.sup.- is a pharmaceutically acceptable anion.

7. 发明申请

US20100029628A1 2,4,5-Substituted Piperidines as Renin Inhibitors 审中-公开
标题翻译： 2,4,5-取代哌啶酮作为肾素抑制剂
公开(公告)号：US20100029628A1
公开(公告)日：2010-02-04
申请号：US11887227
申请日：2006-03-30
申请人： Peter Herold , Robert Mah , Vincenzo Tschinke , Christiane Marti , Stefan Stutz , Stjepan Jelakovic , Zenon D. Konteatis , Jennifer L. Ludington , Michael Quirmbach , Aleksandar Stojanovic , Dirk Behnke , Frank Hollinger
发明人： Peter Herold , Robert Mah , Vincenzo Tschinke , Christiane Marti , Stefan Stutz , Stjepan Jelakovic , Zenon D. Konteatis , Jennifer L. Ludington , Michael Quirmbach , Aleksandar Stojanovic , Dirk Behnke , Frank Hollinger
IPC分类号： A61K31/538 , C07D413/02 , A61P9/00 , A61P13/00
CPC分类号： C07D413/12 , C07D413/14
摘要： SP-P2140 ATE-132—Abstract Novel substituted piperidines of the general formula (I) and (II) with the substituent definitions as explained in detail in the description are described. The compounds are suitable in particular as renin inhibitors and are highly potent.
摘要翻译： SP-P2140ATE-132-摘要描述了通式（I）和（II）的具有取代基定义的新颖取代的哌啶，如在说明书中详细说明的。该化合物特别适合作为肾素抑制剂，并且是非常有效的。

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