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1. 发明授权

US07645754B2 Pyrrolopyrimidine A2B selective antagonist compounds, their synthesis and use 失效
公开(公告)号：US07645754B2
公开(公告)日：2010-01-12
申请号：US10536119
申请日：2007-06-19
申请人： Arlindo Castelhano , Bryan McKibben , Arno Steinig
发明人： Arlindo Castelhano , Bryan McKibben , Arno Steinig
IPC分类号： C07D487/04 , A61K31/519 , A61P11/06
CPC分类号： C07D487/04
摘要： The subject invention provides compounds having the structure: wherein, R1 is a substituted or unsubstituted alkyl, wherein the substituent is hydroxyl, dihydroxy, carboxyl, —C(═O)NRaRb, —NRaRb, —NRaC(═O)NRaRb, —NRaC(═O)ORa, —OC(═O)NRaRb, or —NHC(═O) Ra; R2 is hydrogen or a substituted or unsubstituted alkyl, wherein the substituent is hydroxyl, dihydroxy, carboxyl, —C(═O)NRaRb, —NRaRb, —NRaC(═O)NRaRb, —NRaC(═O)ORa, —OC(═O)NRaRb, or —NHC(═O)Ra, or R1, R2 and N together form a substituted piperazine, substituted azetidine ring, or a pyrrolidine ring substituted with —(CH2)2OH or —CH2C(═O)OH; R3 is a substituted or unsubstituted phenyl or a 5-6 membered heteroaryl ring, wherein the substituent is halogen, hydroxyl, cyano, (C1-C15)alkyl, (C1-C15)alkoxy, or —NRaRb; R4 is hydrogen or substituted or unsubstituted (C1-C15)alkyl; R5 is —(CH2)mOR6, —CHNOR7, —C(═O)NR8R9, —(CH2)mC(═O)OR10, —(CH2)kC(═O)NR11R12; wherein R6 is a substituted or unsubstituted (C1-C30)alkyl, (C3-C10)cycloalkyl, or an aryl, heteroaryl or 4-8 membered heterocyclic ring; R7 is hydrogen, or a substituted or unsubstituted (C1-C30)alkyl, (C1-C30)alkylaryl; R8 and R9 are each independently hydrogen, or a substituted or unsubstituted (C1-C30)alkyl, (C1-C30)alkylaryl, (C1-C30)alkylamino, (C1-C30)alkoxy, or a saturated or unsaturated, monocyclic or bicyclic, carbocyclic or heterocyclic ring, or R8, N, and R9 together form a substituted or unsubstituted 4-8 membered heterocyclic ring; R10 is hydrogen or a substituted or unsubstituted (C1-C30)alkyl, (C3-C10)cycloalkyl, or an aryl, heteroaryl or heterocyclic ring; R11, N and R12 together form a 4-8 membered heterocyclic ring; Ra and Rb are each independently hydrogen or alkyl; m is 0, 1, 2 or 3; and k is 1, 2 or 3, or a specific enantiomer thereof, or a specific tautomer thereof, or a pharmaceutically acceptable salt thereof, and a method for treating a disease associated with the A2b adenosine receptor in a subject in need of such treatment comprising administering to the subject a therapeutically effective amount of the compounds of the invention.

2. 发明授权

US07601714B2 Pyrimidine derivatives useful as inhibitors of PKC-theta 有权
标题翻译：可用作PKC-θ抑制剂的嘧啶衍生物
公开(公告)号：US07601714B2
公开(公告)日：2009-10-13
申请号：US11175476
申请日：2005-07-06
申请人： Antonio J. M. Barbosa, Jr. , Steven Richard Brunette , Eugene Richard Hickey , Jin Mi Kim , Michael David Lawlor , René Marc Lemieux , Bryan McKibben , Matt Aaron Tschantz , Hui Yu
发明人： Antonio J. M. Barbosa, Jr. , Steven Richard Brunette , Eugene Richard Hickey , Jin Mi Kim , Michael David Lawlor , René Marc Lemieux , Bryan McKibben , Matt Aaron Tschantz , Hui Yu
IPC分类号： C07D239/48 , C07D403/12 , A61K31/505
CPC分类号： C07D239/48 , C07D401/12 , C07D403/12
摘要： Disclosed are novel compounds of formula (I): wherein X, Y, R1, R2 and R3 are as defined herein, which are useful as inhibitors of PKC-theta and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC-theta, including immunological disorders and type II diabetes. This invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
摘要翻译：公开了式（I）的新化合物：其中X，Y，R 1，R 2和R 3如本文所定义，其可用作PKC-θ的抑制剂，因此可用于治疗介导的多种疾病和病症通过PKC-θ的活性持续，包括免疫学障碍和II型糖尿病。本发明还涉及包含这些化合物的药物组合物，使用这些化合物治疗各种疾病和病症的方法，制备这些化合物的方法和可用于这些方法的中间体。

3. 发明授权

US07598252B2 Compounds specific to adenosine A, receptors and uses thereof 失效
标题翻译：对腺苷A，受体及其用途具有特异性的化合物
公开(公告)号：US07598252B2
公开(公告)日：2009-10-06
申请号：US10718280
申请日：2003-11-20
申请人： Arlindo L. Castelhano , Bryan McKibben , David J. Witter
发明人： Arlindo L. Castelhano , Bryan McKibben , David J. Witter
IPC分类号： A01N43/54 , A01N43/90
CPC分类号： C07D487/04 , A61K31/519
摘要： This invention pertains to compounds which specifically inhibit the adenosine A1 receptor and the use of these compounds to treat a disease associated with A1 adenosine receptors in a subject.
摘要翻译：本发明涉及特异性抑制腺苷A1受体的化合物以及这些化合物用于治疗受试者中与腺苷受体A1相关的疾病的用途。

4. 发明申请

US20090192177A1 2-ARYL pyrrologpyrimidines for A1 and A3 receptors 审中-公开
标题翻译：用于A1和A3受体的2-ARYL吡咯并嘧啶
公开(公告)号：US20090192177A1
公开(公告)日：2009-07-30
申请号：US12231029
申请日：2008-08-27
申请人： Arlindo L. Castelhano , Bryan McKibben , Douglas S. Werner , David Witter
发明人： Arlindo L. Castelhano , Bryan McKibben , Douglas S. Werner , David Witter
IPC分类号： A61K31/519 , C07D487/04 , A61P11/06 , A61P27/02 , A61P27/06
CPC分类号： C07D487/04
摘要： This invention pertains to compounds which specifically inhibit the adenosine A1 and A3 receptors and the use of these compounds to treat a disease associated with A3 adenosine receptor in a subject, comprising administering to the subject a therapeutically effective amount of the compounds.
摘要翻译：本发明涉及特异性抑制腺苷A1和A3受体的化合物以及这些化合物用于治疗受试者中与A3腺苷受体相关的疾病的用途，其包括向受试者施用治疗有效量的化合物。

5. 发明申请

US20080261943A1 PYRROLOPYRIMIDINE A2B SELECTIVE ANTAGONIST COMPOUNDS, THEIR SYNTHESIS AND USE 失效
公开(公告)号：US20080261943A1
公开(公告)日：2008-10-23
申请号：US10536119
申请日：2007-06-19
申请人： Arlindo Castelhano , Bryan McKibben , Arno Steinig
发明人： Arlindo Castelhano , Bryan McKibben , Arno Steinig
IPC分类号： A61K31/519 , C07D487/04
CPC分类号： C07D487/04
摘要： The subject invention provides compounds having the structure: wherein, R1 is a substituted or unsubstituted alkyl, wherein the substituent is hydroxyl, dihydroxy, carboxyl, —C(═O)NRaRb, —NRaRb, —NRaC(═O)NRaRb, —NRaC(═O)ORa, —OC(═O)NRaRb, or —NH C(═O) Ra; R2 is hydrogen or a substituted or unsubstituted alkyl, wherein the substituent is hydroxyl, dihydroxy, carboxyl, —C(═O)NRaRb, —NRaRb, —NRaC(═O)NRaRb, —NRaC(═O)ORa, —OC(═O)NRaRb, or —NHC(═O)Ra, or R1, R2 and N together form a substituted piperazine, substituted azetidine ring, or a pyrrolidine ring substituted with —(CH2)2OH or —CH2C(═O)OH; R3 is a substituted or unsubstituted phenyl or a 5-6 membered heteroaryl ring, wherein the substituent is halogen, hydroxyl, cyano, (C1-C15)alkyl, (C1-C15)alkoxy, or —NRaRb; R4 is hydrogen or substituted or unsubstituted (C1-C15)alkyl; R5 is —(CH2)mOR6, —CHNOR7, —C(═O)NR8R9, —(CH2)mC(═O)OR10, —(CH2)kC(═O)NR11R12; wherein R6 is a substituted or unsubstituted (C1-C30)alkyl, (C3-C10)cycloalkyl, or an aryl, heteroaryl or 4-8 membered heterocyclic ring; R7 is hydrogen, or a substituted or unsubstituted (C1-C30)alkyl, (C1-C30)alkylaryl; R8 and R9 are each independently hydrogen, or a substituted or unsubstituted (C1-C30)alkyl, (C1-C30)alkylaryl, (C1-C30)alkylamino, (C1-C30)alkoxy, or a saturated or unsaturated, monocyclic or bicyclic, carbocyclic or heterocyclic ring, or R8, N, and R9 together form a substituted or unsubstituted 4-8 membered heterocyclic ring; R10 is hydrogen or a substituted or unsubstituted (C1-C30)alkyl, (C3-C10)cycloalkyl, or an aryl, heteroaryl or heterocyclic ring; R11, N and R12 together form a 4-8 membered heterocyclic ring; Ra and Rb are each independently hydrogen or alkyl; m is 0, 1, 2 or 3; and k is 1, 2 or 3, or a specific enantiomer thereof, or a specific tautomer thereof, or a pharmaceutically acceptable salt thereof, and a method for treating a disease associated with the A2b adenosine receptor in a subject in need of such treatment comprising administering to the subject a therapeutically effective amount of the compounds of the invention.

6. 发明申请

US20080070936A1 Compounds specific to adenosine A1 receptors and uses thereof 审中-公开
标题翻译：对腺苷A1受体特异的化合物及其用途
公开(公告)号：US20080070936A1
公开(公告)日：2008-03-20
申请号：US11903147
申请日：2007-09-20
申请人： Arlindo Castelhano , Bryan McKibben , David Witter
发明人： Arlindo Castelhano , Bryan McKibben , David Witter
IPC分类号： A61K31/519 , A61P11/00 , A61P25/00 , A61P9/00
CPC分类号： C07D487/04 , A61K31/519
摘要： This invention pertains to compounds which specifically inhibit the adenosine A1 receptor and the use of these compounds to treat a disease associated with A1 adenosine receptors in a subject.
摘要翻译：本发明涉及特异性抑制腺苷A 1受体的化合物以及这些化合物用于治疗受试者中Aβ1腺苷受体相关疾病的用途。

7. 发明授权

US07160890B2 Compounds specific to adenosine A3 receptor and uses thereof 失效
标题翻译：对腺苷A3受体特异性的化合物及其用途
公开(公告)号：US07160890B2
公开(公告)日：2007-01-09
申请号：US09728616
申请日：2000-12-01
申请人： Arlindo L. Castelhano , Bryan McKibben , David J. Witter
发明人： Arlindo L. Castelhano , Bryan McKibben , David J. Witter
IPC分类号： A01N43/90 , A61K31/52 , C07D239/00 , C07D487/00
CPC分类号： C07D487/04
摘要： This invention pertains to compounds which specifically inhibit the adenosine A3 receptor and the use of these compounds to treat a disease associated with A3 adenosine receptor in a subject, comprising administering to the subject a therapeutically effective amount of the compounds.
摘要翻译：本发明涉及特异性抑制腺苷A 3受体的化合物和这些化合物用于治疗受试者中与Aβ3腺苷受体相关的疾病的用途，包括给予该受试者治疗有效量的化合物。

8. 发明授权

US06878716B1 Compounds specific to adenosine A1 receptor and uses thereof 失效
标题翻译：对腺苷A1受体特异的化合物及其用途
公开(公告)号：US06878716B1
公开(公告)日：2005-04-12
申请号：US09454074
申请日：1999-12-02
申请人： Arlindo L. Castelhano , Bryan McKibben , David J. Witter
发明人： Arlindo L. Castelhano , Bryan McKibben , David J. Witter
IPC分类号： A61K31/519 , C07D487/04 , A61K31/517 , C07D239/94
CPC分类号： C07D487/04 , A61K31/519
摘要： This invention pertains to compounds which specifically inhibit the adenosine A1 receptor and the use of these compounds to treat a disease associated with A1 adenosine receptor in a subject, comprising administering to the subject a therapeutically effective amount of the compounds.
摘要翻译：本发明涉及特异性抑制腺苷A1受体的化合物以及这些化合物用于治疗受试者中与腺苷受体A1相关的疾病的用途，其包括向受试者施用治疗有效量的化合物。

9. 发明授权

US06673802B2 Compounds specific to adenosine A3 receptor and uses thereof 失效
标题翻译：对腺苷A3受体特异性的化合物及其用途
公开(公告)号：US06673802B2
公开(公告)日：2004-01-06
申请号：US10006405
申请日：2001-11-30
申请人： Arlindo L. Castelhano , Bryan McKibben , David J. Witter
发明人： Arlindo L. Castelhano , Bryan McKibben , David J. Witter
IPC分类号： C07D47334
CPC分类号： C07D487/04 , A61K31/519
摘要： The subject invention provides a compound having the structure: or a pharmaceutically acceptable salt thereof and a method for treating a disease associated with the A3 adenosine receptor by administering a therapeutically effective amount of the compound.
摘要翻译：本发明提供具有以下结构的化合物或其药学上可接受的盐以及通过施用治疗有效量的化合物治疗与A3腺苷受体相关的疾病的方法。

10. 发明授权

US6037340A Synthesis and use of thiophene- and pyrrole-based heteroaromatic compounds 失效
标题翻译：噻吩和吡咯基杂芳族化合物的合成与应用
公开(公告)号：US6037340A
公开(公告)日：2000-03-14
申请号：US864240
申请日：1997-05-28
申请人： Arlindo L. Castelhano , Bryan McKibben
发明人： Arlindo L. Castelhano , Bryan McKibben
IPC分类号： C07B61/00 , C07D333/38 , C07D495/04 , C07D498/04 , A61K31/38 , A61K31/40 , A61K31/435 , C07D205/02
CPC分类号： C07D495/04 , C07D333/38 , C40B40/04 , C40B50/08 , C40B50/14 , C07B2200/11
摘要： Methods for preparing thiophene and pyrrole-based heterocyclic compounds are disclosed. Also disclosed are libraries of thiophene and pyrrole-based heterocyclic compounds, methods for preparing the libraries of thiophene and pyrrole-based heterocyclic compounds, and methods for using the thiophene and pyrrole-based heterocyclic compounds and compound libraries of the invention. The compounds of the invention have biological activity including anti-cancer activity.
摘要翻译：公开了制备噻吩和吡咯基杂环化合物的方法。还公开了噻吩和吡咯基杂环化合物的文库，用于制备噻吩和吡咯基杂环化合物的文库的方法，以及使用本发明的噻吩和吡咯基杂环化合物和化合物文库的方法。本发明的化合物具有包括抗癌活性的生物活性。

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