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1. 发明授权

US5817774A Unsymmetrical complexing agents and targeting immunoreagents useful in therapeutic and diagnostic compositions and methods 失效
标题翻译：用于治疗和诊断组合物和方法的不对称络合剂和靶向免疫反应剂
公开(公告)号：US5817774A
公开(公告)日：1998-10-06
申请号：US719407
申请日：1996-09-24
申请人： Daniel J. Delecki , Ashis Kumar Saha , Robert A. Snow
发明人： Daniel J. Delecki , Ashis Kumar Saha , Robert A. Snow
IPC分类号： A61K47/48 , A61K51/04 , A61K51/10 , C07D213/26 , C07D213/30 , C07D213/48 , C07D213/56 , C07D213/61 , C07D213/74 , C07D213/75 , C07D213/84 , C07F13/00
CPC分类号： C07D213/84 , A61K47/48707 , A61K51/0478 , A61K51/1093 , C07D213/26 , C07D213/30 , C07D213/48 , C07D213/56 , C07D213/61 , C07D213/74 , C07D213/75 , A61K2121/00 , A61K2123/00
摘要： Described are novel, unsymmetrical oligo-2,6-pyridine complexing agents. Also described are metal chelates and targeting immunoreagents containing such completing agents as well as diagnostic and therapeutic compositions containing such immunoreagents and diagnostic and therapeutic methods of using the immunoreagents.
摘要翻译：描述的是新型的，不对称的低聚-2,6-吡啶络合剂。还描述了含有这种完成剂的金属螯合物和靶向免疫反应剂以及含有这种免疫反应剂的诊断和治疗组合物以及使用免疫反应剂的诊断和治疗方法。

2. 发明申请

US20100168080A1 NOVEL COMPOUNDS USEFUL AS CC CHEMOKINE RECEPTOR LIGANDS 审中-公开
标题翻译：新化合物作为CC CHEMOKINE RECEPTOR LIGANDS有用
公开(公告)号：US20100168080A1
公开(公告)日：2010-07-01
申请号：US12639297
申请日：2009-12-16
申请人： Uttam KHAMRAI , Sumit Kumar Karak , Matthew Ronsheim , Ashis Kumar Saha
发明人： Uttam KHAMRAI , Sumit Kumar Karak , Matthew Ronsheim , Ashis Kumar Saha
IPC分类号： C07D265/30 , A61K31/553 , C07D211/06 , A61K31/5375 , C07D491/00 , A61K31/437 , C07D267/10 , C07D413/06 , C07D498/02 , A61K31/445 , A61P3/06 , A61P29/00
CPC分类号： C07D267/10 , A61K31/437 , A61K31/445 , A61K31/5375 , A61K31/553 , C07D207/12 , C07D211/48 , C07D211/54 , C07D211/62 , C07D265/30 , C07D401/06 , C07D401/12 , C07D413/06 , C07D413/12 , C07D498/10
摘要： The present invention relates to novel morpholine, oxazapane and piperidine derivatives that act as ligands for CC chemokine receptors, such as CCR1. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.
摘要翻译：本发明涉及作为CC趋化因子受体如CCR1的配体的新型吗啉，恶唑烷和哌啶衍生物。本发明还涉及制备化合物的方法，含有该化合物的组合物以及使用该化合物的治疗方法。

3. 发明授权

US5892024A Bifunctional nucleosides, oligomers thereof, and methods of making and using the same 失效
标题翻译：双功能核苷，其低聚物及其制备和使用方法
公开(公告)号：US5892024A
公开(公告)日：1999-04-06
申请号：US816708
申请日：1997-03-13
申请人： Prasad Venkata Chala Chaturvedula , Ashis Kumar Saha
发明人： Prasad Venkata Chala Chaturvedula , Ashis Kumar Saha
IPC分类号： C12N15/09 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61K31/708 , A61K31/7088 , A61P31/12 , A61P35/00 , C07H19/04 , C07H19/06 , C07H19/16 , C07H21/00 , C07H21/02 , C07H21/04 , C07H19/067 , C07H19/073 , C07H19/167 , C07H19/173
CPC分类号： C07H21/00 , C07H19/04
摘要： Disclosed are novel bifunctional nucleoside analogs and oligonucleosides of 3-4 bases (trimers and tetramers) and longer containing at least two consecutive internucleoside linkages of two carbon-one nitrogen atom or two carbon-one oxygen atom (3'-NCC-5', 3'-CNC-5', 3'-OCC-5') internucleoside linkages. The bifunctional nucleosides are useful for preparing the trimers and tetramers, which, in turn, are useful, together with the nucleosides, in preparing oligonucleosides as well as chimeric oligonucleotide analogs, preferably antisense oligonucleosides and oligonucleotide analogs, of 6 to about 60 bases having at least two consecutive internucleoside linkages of two carbon atoms and one nitrogen atom or 2 carbon atoms and one oxygen atom in the oligonucleoside backbone.
摘要翻译：公开了具有3-4个碱基（三聚体和四聚体）和更长的包含两个碳一氮原子或两个碳一氧原子的至少两个连续核苷键的新型双功能核苷类似物和寡核苷酸（3'-NCC-5' 3'-CNC-5'，3'-OCC-5'）核苷间键。双功能核苷可用于制备三聚体和四聚体，其又可与核苷一起制备寡核苷酸以及嵌合寡核苷酸类似物，优选反义寡核苷酸和寡核苷酸类似物，其具有6至约60个碱基，其具有寡核苷酸主链中两个碳原子和一个氮原子或2个碳原子和一个氧原子的至少两个连续的核苷间键。

4. 发明授权

US07592356B2 Triazoles as farnesyl transferase inhibitors 有权
标题翻译：三唑作为法呢基转移酶抑制剂
公开(公告)号：US07592356B2
公开(公告)日：2009-09-22
申请号：US11926858
申请日：2007-10-29
申请人： Ashis Kumar Saha , David William End , Bart Lieven Daniel De Corte , Henry Joseph Breslin , Li Liu
发明人： Ashis Kumar Saha , David William End , Bart Lieven Daniel De Corte , Henry Joseph Breslin , Li Liu
IPC分类号： A61K31/47 , C07D249/08
CPC分类号： C07D249/08 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D417/12
摘要： a prodrug, N-oxide, addition salt, quaternary amine or stereochemically isomeric form thereof, wherein L1 and L2 are R1—Y— wherein each (R1—Y)— substituent is defined independently of the other; Y is C1-4alkanediyl, C2-4alkenediyl, C2-4alkynediyl, C(═O), or a direct bond; R1 is hydrogen, cyano, aryl or a substituted or unsubstituted C1-14heterocycle; ═Z1—Z2═Z3— represents a radical of formula ═N—N═CH— (a-1), ═N—CH═N— (a-2), ═CH—N═N— (a-3); X is SO2, (CH2), wherein n is 1 to 4, C(═O), C(═S), or a direct bond; R2 is aryl, C3-7cycloalkyl, C3-7cycloalkyl substituted with one or more substituents independently selected from hydroxy, aryl, aryloxy, a substituted or unsubstituted C1-14heterocycle, C3-7cycloalkyl, hydroxycarbonyl, C1-6alkyloxycarbonyl, hydroxyC1-6alkyl, hydroxyC1-6alkyloxy, hydroxyC1-6alkylthio and arylC1-6alkylthio, C1-12alkyl or C1-12alkyl substituted with one or more substituents independently selected from hydroxy, aryl, aryloxy, a substituted or unsubstituted C1-14heterocycle, C3-7cycloalkyl, hydroxycarbonyl, C1-6alkyloxycarbonyl, hydroxyC1-6alkyl, hydroxyC1-6alkyloxy, hydroxyC1-6alkylthio and arylC1-6alkylthio; R3 is aryl, —NR5R6, a substituted or unsubstituted C1-14heterocycle, or C2-4alkenediyl substituted with a substituted or unsubstituted C1-14heterocycle or aryl; R4 is hydrogen, aryl, C3-7cycloalkyl, C1-6alkyl or C1-6alkyl substituted with C3-7cycloalkyl, hydroxycarbonyl, C1-4alkyloxycarbonyl or aryl; R5 and R6 are each independently selected from hydrogen, a substituted or unsubstituted C1-14heterocycle, aryl, C1-12alkyl and C1-12alkyl substituted with one or more substituents selected from hydroxy, aryl, aryloxy or a substituted or unsubstituted C1-14heterocycle.
摘要翻译：前药，N-氧化物，加成盐，季胺或其立体化学异构形式，其中L 1和L 2是R 1 -Y-，其中每个（R 1 -Y） - 取代基独立地彼此定义; Y是C1-4烷二基，C2-4亚烯基，C2-4炔二基，C（-O）或直接键; R1是氢，氰基，芳基或取代或未取代的C1-14杂环; -Z1-Z2-Z3-表示式-N-N-CH-（a-1），-N-CH-N-（a-2），-CH-N-N-（a-3） X是SO 2，（CH 2），其中n是1至4，C（-O），C（-S）或直接键; R 2是芳基，C 3-7环烷基，被一个或多个独立地选自羟基，芳基，芳氧基，取代或未取代的C 1-14杂环，C 3-7环烷基，羟基羰基，C 1-6烷氧基羰基，羟基C 1-6烷基，羟基C 1-6烷基，被一个或多个独立地选自羟基，芳基，芳氧基，取代或未取代的C 1-14杂环，C 3-7环烷基，羟基羰基，C 1-6烷氧基羰基，C 1-6烷氧基羰基，C 1-6烷硫基，羟基C 1-6烷基，羟基C 1-6烷氧基，羟基C 1-6烷硫基和芳基C 1-6烷硫基; R3是芳基，-NR5R6，取代或未取代的C1-14杂环，或被取代或未取代的C1-14杂环或芳基取代的C2-4亚烯基; R4是氢，芳基，C3-7环烷基，C1-6烷基或被C3-7环烷基取代的C1-6烷基，羟基羰基，C1-4烷氧基羰基或芳基; R 5和R 6各自独立地选自氢，取代或未取代的C 1-14杂环，芳基，C 1-12烷基和被一个或多个选自羟基，芳基，芳氧基或取代或未取代的C 1-14杂环的取代基取代的C 1-12烷基。

5. 发明授权

US07511061B2 Triazoles as farnesyl transferase inhibitors 有权
标题翻译：三唑作为法呢基转移酶抑制剂
公开(公告)号：US07511061B2
公开(公告)日：2009-03-31
申请号：US11143814
申请日：2005-06-02
申请人： Ashis Kumar Saha , David William End , Bart Lieven Daniel De Corte , Henry Joseph Breslin , Li Liu
发明人： Ashis Kumar Saha , David William End , Bart Lieven Daniel De Corte , Henry Joseph Breslin , Li Liu
IPC分类号： A61K31/4196 , A61K31/47 , C07D215/00 , C07D249/06
CPC分类号： C07D249/08 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D417/12
摘要： A prodrug, N-oxide, addition salt, quaternary amine or stereochemically isomeric form thereof, wherein L1 and L2 are R1—Y— wherein each (R1—Y)— substituent is defined independently of the other; Y is C1-4alkanediyl, C2-4alkenediyl, C2-4alkynediyl, C(═O), or a direct bond; R1 is hydrogen, cyano, aryl or a substituted or unsubstituted C1-14heterocycle; =Z1-Z2=Z3- represents a radical of formula ═N—N═CH— (a-1), ═N—CH═N— (a-2), ═CH—N═N— (a-3); X is SO2, (CH2)n wherein n is 1 to 4, C(═O), C(═S), or a direct bond; R2 is aryl, C3-7cycloalkyl, C3-7cycloalkyl substituted with one or more substituents independently selected from hydroxy, aryl, aryloxy, a substituted or unsubstituted C1-14heterocycle, C3-7cycloalkyl, hydroxycarbonyl, C1-6alkyloxycarbonyl, hydroxyC1-6alkyl, hydroxyC1-6alkyloxy, hydroxyC1-6alkylthio and arylC1-6alkylthio, C1-12alkyl or C1-12alkyl substituted with one or more substituents independently selected from hydroxy, aryl, aryloxy, a substituted or unsubstituted C1-14heterocycle, C3-7cycloalkyl, hydroxycarbonyl, C1-6alkyloxycarbonyl, hydroxyC1-6alkyl, hydroxyC1-6alkyloxy, hydroxyC1-6alkylthio and arylC1-6alkylthio; R3 is aryl, —NR5R6, a substituted or unsubstituted C1-14heterocycle, or C2-4alkenediyl substituted with a substituted or unsubstituted C1-14heterocycle or aryl; R4 is hydrogen, aryl, C3-7cycloalkyl, C1-6alkyl or C1-6alkyl substituted with C3-7cycloalkyl, hydroxycarbonyl, C1-4alkyloxycarbonyl or aryl; R5 and R6 are each independently selected from hydrogen, a substituted or unsubstituted C1-14heterocycle, aryl, C1-12alkyl and C1-12alkyl substituted with one or more substituents selected from hydroxy, aryl, aryloxy or a substituted or unsubstituted C1-14heterocycle.
摘要翻译：前药，N-氧化物，加成盐，季胺或其立体化学异构形式，其中L 1和L 2是R 1 -Y-，其中每个（R 1 -Y） - 取代基独立地彼此定义; Y是C1-4烷二基，C2-4亚烯基，C2-4炔二基，C（-O）或直接键; R1是氢，氰基，芳基或取代或未取代的C1-14杂环; = Z1-Z2 = Z3-表示式-N-N-CH-（a-1），-N-CH-N-（a-2），-CH-N-N-（a-3） X是SO 2，（CH 2）n，其中n是1至4，C（-O），C（-S）或直接键; R 2是芳基，C 3-7环烷基，被一个或多个独立地选自羟基，芳基，芳氧基，取代或未取代的C 1-14杂环，C 3-7环烷基，羟基羰基，C 1-6烷氧基羰基，羟基C 1-6烷基，羟基C 1-6烷基，被一个或多个独立地选自羟基，芳基，芳氧基，取代或未取代的C 1-14杂环，C 3-7环烷基，羟基羰基，C 1-6烷氧基羰基，C 1-6烷氧基羰基，C 1-6烷硫基，羟基C 1-6烷基，羟基C 1-6烷氧基，羟基C 1-6烷硫基和芳基C 1-6烷硫基; R3是芳基，-NR5R6，取代或未取代的C1-14杂环，或被取代或未取代的C1-14杂环或芳基取代的C2-4亚烯基; R4是氢，芳基，C3-7环烷基，C1-6烷基或被C3-7环烷基取代的C1-6烷基，羟基羰基，C1-4烷氧基羰基或芳基; R 5和R 6各自独立地选自氢，取代或未取代的C 1-14杂环，芳基，C 1-12烷基和被一个或多个选自羟基，芳基，芳氧基或取代或未取代的C 1-14杂环的取代基取代的C 1-12烷基。

6. 发明授权

US07173040B2 Farnesyl transferase inhibiting 6-[(substituted phenyl)methyl]-quinoline and quinazoline derinazoline derivatives 有权
标题翻译：法呢基转移酶抑制6 - [（取代苯基）甲基] - 喹啉和喹唑啉衍生物衍生物
公开(公告)号：US07173040B2
公开(公告)日：2007-02-06
申请号：US10381556
申请日：2001-09-18
申请人： Patrick René Angibaud , Marc Gaston Venet , Ashis Kumar Saha , Laurence Anne Mevellec
发明人： Patrick René Angibaud , Marc Gaston Venet , Ashis Kumar Saha , Laurence Anne Mevellec
IPC分类号： C07D403/06 , A61K31/47 , C07D215/227
CPC分类号： C07D401/06 , C07D401/14 , C07D403/06 , C07D405/14 , C07D413/14 , C07D417/14 , C07D487/04
摘要： This invention comprises the compounds of formula (I): wherein r, s, t, Y1–Y2, R1, R2, R3, R4, R5, R6 and R7 have defined meanings, having farnesyl transferase inhibiting activity; their preparation, compositions containing them and their use as a medicine.
摘要翻译：本发明包括式（I）化合物：其中r，s，t，Y 1 -Y 2，R 1，R 2， R 2，R 3，R 4，R 5，R 6和R 6， SUP> 7限定含义，具有法呢基转移酶抑制活性; 其制剂，含有它们的组合物及其作为药物的用途。

7. 发明授权

US07049324B1 Triazoles as farnesyl transferase inhibitors 有权
公开(公告)号：US07049324B1
公开(公告)日：2006-05-23
申请号：US10130322
申请日：2000-11-15
申请人： Ashis Kumar Saha , David William End , Bart Lieven Daniel De Corte , Henry Joseph Breslin , Li Liu
发明人： Ashis Kumar Saha , David William End , Bart Lieven Daniel De Corte , Henry Joseph Breslin , Li Liu
IPC分类号： A61K31/47 , C07D215/38 , C07D249/08
CPC分类号： C07D249/08 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D417/12 , C07D487/14
摘要： a prodrug, N-oxide, addition salt, quaternary amine or stereochemically isomeric form thereof, wherein L1 and L2 are R1—Y— wherein each (R1—Y)— substituent is defined independently of the other; Y is C1-4alkanediyl, C2-4alkenediyl, C2-4alkynediyl, C(═O), or a direct bond; R1 is hydrogen, cyano, aryl or a substituted or unsubstituted C1-14heterocycle; ═Z1—Z2═Z3— represents a radical of formula ═N—N═CH— (a-1), ═N—CH═N— (a-2), ═CH—N═N— (a-3); X is SO2, (CH2)n wherein n is 1 to 4, C(═O), C(═S), or a direct bond, R2 is aryl, C3-7cycloalkyl, C3-7cycloalkyl substituted with one or more substituents independently selected from hydroxy, aryl, aryloxy, a substituted or unsubstituted C1-14heterocycle, C3-7cycloalkyl, hydroxycarbonyl, C1-6alkyloxycarbonyl, hydroxyC1-6alkyl, hydroxyC1-6alkyloxy, hydroxyC1-6alkylthio and arylC1-6alkylthio, C1-12alkyl or C1-12alkyl substituted with one or more substituents independently selected from hydroxy, aryl, aryloxy, a substituted or unsubstituted C1-14heterocycle, C3-7cycloalkyl, hydroxycarbonyl, C1-6alkyloxycarbonyl, hydroxyC1-6alkyl, hydroxyC1-6alkyloxy, hydroxyC1-6alkylthio and arylC1-6alkylthio; R3 is aryl, —NR5R6, a substituted or unsubstituted C1-14heterocycle, or C2-4alkenediyl substituted with a substituted or unsubstituted C1-14heterocycle or aryl; R4 is hydrogen, aryl, C3-7cycloalkyl, C1-6alkyl or C1-6alkyl substituted with C3-7cycloalkyl, hydroxycarbonyl, C1-4alkyloxycarbonyl or aryl; R5 and R6 are each independently selected from hydrogen, a substituted or unsubstituted C1-14heterocycle, aryl, C1-12alkyl and C1-12alkyl substituted with one or more substituents selected from hydroxy, aryl, aryloxy or a substituted or unsubstituted C1-14heterocycle.

8. 发明授权

US06248870B1 Unsymmetrical complexing agents and targeting immunoreagents useful in therapeutic and diagnostic compositions and methods 失效
标题翻译：用于治疗和诊断组合物和方法的不对称络合剂和靶向免疫反应剂
公开(公告)号：US06248870B1
公开(公告)日：2001-06-19
申请号：US09139364
申请日：1998-08-25
申请人： Daniel J. Delecki , Ashis Kumar Saha , Robert A. Snow
发明人： Daniel J. Delecki , Ashis Kumar Saha , Robert A. Snow
IPC分类号： C07F2155
CPC分类号： C07D213/84 , A61K47/6887 , A61K51/0478 , A61K51/1093 , A61K2121/00 , A61K2123/00 , C07D213/26 , C07D213/30 , C07D213/48 , C07D213/56 , C07D213/61 , C07D213/74 , C07D213/75
摘要： A method for diagnostic imaging a site in a patient. The method involves the use of an immunoreactive group which is linked to an unsymmetrical oligo-2,6-pyrimidine complexing agent.
摘要翻译：一种用于对患者中的部位进行诊断成像的方法。该方法涉及使用与不对称寡聚-2,6-嘧啶络合剂连接的免疫反应性基团。

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