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1. 发明授权

US07429604B2 Six-membered heterocycles useful as serine protease inhibitors 有权
标题翻译：用作丝氨酸蛋白酶抑制剂的六元杂环
公开(公告)号：US07429604B2
公开(公告)日：2008-09-30
申请号：US11151627
申请日：2005-06-13
申请人： James R. Corte , Jon J. Hangeland , Miml L. Quan , Joanne M. Smallheer , Tianan Fang
发明人： James R. Corte , Jon J. Hangeland , Miml L. Quan , Joanne M. Smallheer , Tianan Fang
IPC分类号： A61K31/44 , C07D211/82 , C07D401/02
CPC分类号： C07D401/10 , C07D213/40 , C07D213/55 , C07D213/56 , C07D213/57 , C07D213/61 , C07D213/64 , C07D213/73 , C07D213/74 , C07D213/89 , C07D239/26 , C07D401/04 , C07D401/12 , C07D401/14 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/14
摘要： The present invention provides compounds of Formula (I): or a stereoisomer or pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, X1, X2, X3, X4, and X5 are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
摘要翻译：本发明提供式（I）化合物或其立体异构体或药学上可接受的盐或溶剂合物形式，其中变量A，L，Z，X 1，X 2 >，X 3，X 4和X 5如本文所定义。式（I）的化合物可用作凝血级联和/或接触激活系统的丝氨酸蛋白酶的选择性抑制剂; 例如凝血酶，因子Xa，因子XIa，因子IXa，因子VIIa和/或血浆激肽释放酶。特别地，它涉及作为选择性因子XIa抑制剂的化合物。本发明还涉及包含这些化合物的药物组合物和使用其制备血栓栓塞和/或炎症性疾病的方法。

2. 发明授权

US07453002B2 Five-membered heterocycles useful as serine protease inhibitors 有权
标题翻译：用作丝氨酸蛋白酶抑制剂的五元杂环
公开(公告)号：US07453002B2
公开(公告)日：2008-11-18
申请号：US11151667
申请日：2005-06-13
申请人： Jon J. Hangeland , Mimi L. Quan , Joanne M. Smallheer , Gregory S. Bisacchi , James R. Corte , Todd J. Friends , Zhong Sun , Karen A. Rossi , Cullen L. Cavallaro
发明人： Jon J. Hangeland , Mimi L. Quan , Joanne M. Smallheer , Gregory S. Bisacchi , James R. Corte , Todd J. Friends , Zhong Sun , Karen A. Rossi , Cullen L. Cavallaro
IPC分类号： A61K31/4178 , C07D403/04
CPC分类号： C07D417/14 , C07D231/12 , C07D233/64 , C07D233/68 , C07D233/90 , C07D235/08 , C07D235/14 , C07D235/16 , C07D249/08 , C07D249/12 , C07D263/12 , C07D263/14 , C07D263/32 , C07D277/30 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/10 , C07D413/14 , C07D417/04 , C07D417/06
摘要： The present invention provides a method for treating a thrombotic or an inflammatory disorder administering to a patient in need thereof a therapeutically effective amount of at least one compound of Formula (I) or Formula (V): or a stereoisomer or pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, R3, R4, R6, R11, X1, X2, and X3 are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also provides compounds within the scope of Formula I and relates to pharmaceutical compositions comprising these compounds.
摘要翻译：本发明提供了治疗有需要的患者治疗有效量的至少一种式（I）或式（V）化合物或其立体异构体或药学上可接受的盐或溶剂化物的血栓形成或炎性病症的方法：其形式，其中变量A，L，Z，R 3，R 4，R 6，R 11， >，X 1，X 2和X 3如本文所定义。式（I）的化合物可用作凝血级联和/或接触激活系统的丝氨酸蛋白酶的选择性抑制剂; 例如凝血酶，因子Xa，因子XIa，因子IXa，因子VIIa和/或血浆激肽释放酶。特别地，它涉及作为选择性因子XIa抑制剂的化合物。本发明还提供了式I范围内的化合物，涉及包含这些化合物的药物组合物。

3. 发明授权

US08716492B2 Five-membered heterocycles useful as serine protease inhibitors 有权
标题翻译：用作丝氨酸蛋白酶抑制剂的五元杂环
公开(公告)号：US08716492B2
公开(公告)日：2014-05-06
申请号：US13326809
申请日：2011-12-15
申请人： Jon J. Hangeland , Mimi L. Quan , Joanne M. Smallheer , Gregory S. Bisacchi , James R. Corte , Todd J. Friends , Zhong Sun , Karen A. Rossi , Cullen L. Cavallaro
发明人： Jon J. Hangeland , Mimi L. Quan , Joanne M. Smallheer , Gregory S. Bisacchi , James R. Corte , Todd J. Friends , Zhong Sun , Karen A. Rossi , Cullen L. Cavallaro
IPC分类号： A61K31/5513 , A61K31/423 , A61K31/4178 , A61K31/4725 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D409/14 , C07D413/14
CPC分类号： C07D417/14 , C07D231/12 , C07D233/64 , C07D233/68 , C07D233/90 , C07D235/08 , C07D235/14 , C07D235/16 , C07D249/08 , C07D249/12 , C07D263/12 , C07D263/14 , C07D263/32 , C07D277/30 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/10 , C07D413/14 , C07D417/04 , C07D417/06
摘要： The present invention provides a method for treating a thrombotic or an inflammatory disorder administering to a patient in need thereof a therapeutically effective amount of at least one compound of Formula (I) or Formula (V): or a stereoisomer or pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, R3, R4, R6, R11, X1, X2, and X3 are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also provides compounds within the scope of Formula I and relates to pharmaceutical compositions comprising these compounds.
摘要翻译：本发明提供了治疗有需要的患者治疗有效量的至少一种式（I）或式（V）化合物或其立体异构体或药学上可接受的盐或溶剂化物的血栓形成或炎性病症的方法：其中变量A，L，Z，R3，R4，R6，R11，X1，X2和X3如本文所定义。式（I）的化合物可用作凝血级联和/或接触激活系统的丝氨酸蛋白酶的选择性抑制剂; 例如凝血酶，因子Xa，因子XIa，因子IXa，因子VIIa和/或血浆激肽释放酶。特别地，它涉及作为选择性因子XIa抑制剂的化合物。本发明还提供了式I范围内的化合物，涉及包含这些化合物的药物组合物。

4. 发明申请

US20120088758A1 FIVE-MEMBERED HETEROCYCLES USEFUL AS SERINE PROTEASE INHIBITORS 有权
标题翻译：作为丝氨酸蛋白酶抑制剂有用的五分子杂环化合物
公开(公告)号：US20120088758A1
公开(公告)日：2012-04-12
申请号：US13326809
申请日：2011-12-15
申请人： Jon J. Hangeland , Mimi L. Quan , Joanne M. Smallheer , Gregory S. Bisacchi , James R. Corte , Todd J. Friends , Zhong Sun , Karen A. Rossi , Cullen L. Cavallaro
发明人： Jon J. Hangeland , Mimi L. Quan , Joanne M. Smallheer , Gregory S. Bisacchi , James R. Corte , Todd J. Friends , Zhong Sun , Karen A. Rossi , Cullen L. Cavallaro
IPC分类号： A61K31/5513 , C07D403/14 , C07D413/14 , C07D405/14 , C07D401/14 , C07D401/12 , C07D403/10 , C07D403/12 , A61K31/417 , A61K31/4178 , A61K31/423 , A61K31/4725 , A61K31/4439 , A61K31/517 , A61P7/00 , A61P9/00 , A61P9/06 , A61P9/10 , A61P7/02 , C07D233/64
CPC分类号： C07D417/14 , C07D231/12 , C07D233/64 , C07D233/68 , C07D233/90 , C07D235/08 , C07D235/14 , C07D235/16 , C07D249/08 , C07D249/12 , C07D263/12 , C07D263/14 , C07D263/32 , C07D277/30 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/10 , C07D413/14 , C07D417/04 , C07D417/06
摘要： The present invention provides a method for treating a thrombotic or an inflammatory disorder administering to a patient in need thereof a therapeutically effective amount of at least one compound of Formula (I) or Formula (V): or a stereoisomer or pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, R3, R4, R6, R11, X1, X2, and X3 are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also provides compounds within the scope of Formula I and relates to pharmaceutical compositions comprising these compounds.
摘要翻译：本发明提供了治疗有需要的患者治疗有效量的至少一种式（I）或式（V）化合物或其立体异构体或药学上可接受的盐或溶剂化物的血栓形成或炎性病症的方法：其中变量A，L，Z，R3，R4，R6，R11，X1，X2和X3如本文所定义。式（I）的化合物可用作凝血级联和/或接触激活系统的丝氨酸蛋白酶的选择性抑制剂; 例如凝血酶，因子Xa，因子XIa，因子IXa，因子VIIa和/或血浆激肽释放酶。特别地，它涉及作为选择性因子XIa抑制剂的化合物。本发明还提供了式I范围内的化合物，涉及包含这些化合物的药物组合物。

5. 发明授权

US08101778B2 Five-membered heterocycles useful as serine protease inhibitors 有权
标题翻译：用作丝氨酸蛋白酶抑制剂的五元杂环
公开(公告)号：US08101778B2
公开(公告)日：2012-01-24
申请号：US12209235
申请日：2008-09-12
申请人： Jon J. Hangeland , Mimi L. Quan , Joanne M. Smallheer , Gregory S. Bisacchi , James R. Corte , Todd J. Friends , Zhong Sun , Karen A. Rossi , Cullen L. Cavallaro
发明人： Jon J. Hangeland , Mimi L. Quan , Joanne M. Smallheer , Gregory S. Bisacchi , James R. Corte , Todd J. Friends , Zhong Sun , Karen A. Rossi , Cullen L. Cavallaro
IPC分类号： A61K31/4178 , C07D403/04
CPC分类号： C07D417/14 , C07D231/12 , C07D233/64 , C07D233/68 , C07D233/90 , C07D235/08 , C07D235/14 , C07D235/16 , C07D249/08 , C07D249/12 , C07D263/12 , C07D263/14 , C07D263/32 , C07D277/30 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/10 , C07D413/14 , C07D417/04 , C07D417/06
摘要： The present invention provides a method for treating a thrombotic or an inflammatory disorder administering to a patient in need thereof a therapeutically effective amount of at least one compound of Formula (I) or Formula (V): or a stereoisomer or pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, R3, R4, R6, R11, X1, X2, and X3 are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also provides compounds within the scope of Formula I and relates to pharmaceutical compositions comprising these compounds.
摘要翻译：本发明提供了治疗有需要的患者治疗有效量的至少一种式（I）或式（V）化合物或其立体异构体或药学上可接受的盐或溶剂化物的血栓形成或炎性病症的方法：其中变量A，L，Z，R3，R4，R6，R11，X1，X2和X3如本文所定义。式（I）的化合物可用作凝血级联和/或接触激活系统的丝氨酸蛋白酶的选择性抑制剂; 例如凝血酶，因子Xa，因子XIa，因子IXa，因子VIIa和/或血浆激肽释放酶。特别地，它涉及作为选择性因子XIa抑制剂的化合物。本发明还提供了式I范围内的化合物，涉及包含这些化合物的药物组合物。

6. 发明申请

US20090036438A1 FIVE-MEMBERED HETEROCYCLES USEFUL AS SERINE PROTEASE INHIBITORS 有权
标题翻译：作为丝氨酸蛋白酶抑制剂有用的五分子杂环化合物
公开(公告)号：US20090036438A1
公开(公告)日：2009-02-05
申请号：US12209235
申请日：2008-09-12
申请人： Jon J. Hangeland , Mimi L. Quan , Joanne M. Smallheer , Gregory S. Bisacchi , James R. Corte , Todd J. Friends , Zhong Sun , Karen A. Rossi , Cullen L. Cavallaro
发明人： Jon J. Hangeland , Mimi L. Quan , Joanne M. Smallheer , Gregory S. Bisacchi , James R. Corte , Todd J. Friends , Zhong Sun , Karen A. Rossi , Cullen L. Cavallaro
IPC分类号： A61K31/538 , A61K31/4178 , C07D403/02 , A61K31/517 , A61P7/02 , C07D403/10 , C07D413/10
CPC分类号： C07D417/14 , C07D231/12 , C07D233/64 , C07D233/68 , C07D233/90 , C07D235/08 , C07D235/14 , C07D235/16 , C07D249/08 , C07D249/12 , C07D263/12 , C07D263/14 , C07D263/32 , C07D277/30 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/10 , C07D413/14 , C07D417/04 , C07D417/06
摘要： The present invention provides a method for treating a thrombotic or an inflammatory disorder administering to a patient in need thereof a therapeutically effective amount of at least one compound of Formula (I) or Formula (V): or a stereoisomer or pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, R3, R4, R6, R11, X1, X2, and X3 are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also provides compounds within the scope of Formula I and relates to pharmaceutical compositions comprising these compounds.
摘要翻译：本发明提供了治疗有需要的患者治疗有效量的至少一种式（I）或式（V）化合物或其立体异构体或药学上可接受的盐或溶剂化物的血栓形成或炎性病症的方法：其中变量A，L，Z，R3，R4，R6，R11，X1，X2和X3如本文所定义。式（I）的化合物可用作凝血级联和/或接触激活系统的丝氨酸蛋白酶的选择性抑制剂; 例如凝血酶，因子Xa，因子XIa，因子IXa，因子VIIa和/或血浆激肽释放酶。特别地，它涉及作为选择性因子XIa抑制剂的化合物。本发明还提供了式I范围内的化合物，涉及包含这些化合物的药物组合物。

7. 发明授权

US07709646B2 Tetrahydroquinoline derivatives useful as serine protease inhibitors 有权
标题翻译：用作丝氨酸蛋白酶抑制剂的四氢喹啉衍生物
公开(公告)号：US07709646B2
公开(公告)日：2010-05-04
申请号：US11430588
申请日：2006-05-09
申请人： Mimi L. Quan , Cailan Wang , Jinglan Zhou , Jon J. Hangeland , Dietmar A. Seiffert , Robert M. Knabb
发明人： Mimi L. Quan , Cailan Wang , Jinglan Zhou , Jon J. Hangeland , Dietmar A. Seiffert , Robert M. Knabb
IPC分类号： C07D215/38
CPC分类号： C07D401/12 , C07D215/12 , C07D215/20 , C07D215/48
摘要： The present invention provides compounds of Formula (I): or a stereoisomer or pharmaceutically acceptable salt form thereof, wherein the variables A, B, L1, L2, X1, X2, X3, X4, R4, R5, R13, R14, R15 and R16 are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
摘要翻译：本发明提供式（I）化合物或其立体异构体或药学上可接受的盐形式，其中变量A，B，L1，L2，X1，X2，X3，X4，R4，R5，R13，R14，R15和 R 16如本文所定义。式（I）的化合物可用作凝血级联和/或接触激活系统的丝氨酸蛋白酶的选择性抑制剂; 例如凝血酶，因子Xa，因子XIa，因子IXa，因子VIIa和/或血浆激肽释放酶。特别地，它涉及作为选择性因子XIa抑制剂的化合物。本发明还涉及包含这些化合物的药物组合物和使用其制备血栓栓塞和/或炎症性疾病的方法。

8. 发明授权

US07557143B2 Thyroid receptor ligands 失效
标题翻译：甲状腺受体配体
公开(公告)号：US07557143B2
公开(公告)日：2009-07-07
申请号：US10826100
申请日：2004-04-15
申请人： Denis E. Ryono , Jon J. Hangeland , Todd J. Friends , Tamara Dejneka , Pratik Devasthale , Yolanda V. Caringal , Minsheng Zhang , Arthur M. P. Doweyko , Johan Malm , Andrei Sanin
发明人： Denis E. Ryono , Jon J. Hangeland , Todd J. Friends , Tamara Dejneka , Pratik Devasthale , Yolanda V. Caringal , Minsheng Zhang , Arthur M. P. Doweyko , Johan Malm , Andrei Sanin
IPC分类号： A61K31/165 , A61K31/19 , C07C239/00 , C07C325/00 , C07C229/00 , C07C59/00
CPC分类号： C07C311/46 , A61K31/4439 , A61K31/662 , A61K45/06 , C07C43/29 , C07C43/295 , C07C59/68 , C07C59/72 , C07C65/24 , C07C65/26 , C07C69/16 , C07C69/736 , C07C69/94 , C07C205/38 , C07C217/58 , C07C233/29 , C07C235/34 , C07C235/42 , C07C235/46 , C07C235/52 , C07C235/60 , C07C235/62 , C07C235/64 , C07C311/37 , C07C2601/02 , C07C2601/14 , C07C2602/08 , C07C2603/18 , C07D213/30 , C07D239/26 , C07D257/04 , C07D263/14 , C07D263/32 , C07D277/24 , C07D285/06 , C07D307/42 , C07D307/52 , C07D307/87 , C07D317/58 , C07D317/60 , C07D333/32 , C07F9/306 , C07F9/3241 , C07F9/4056 , A61K2300/00
摘要： Thyroid receptor ligands are provided which have the general formula I wherein: R1 is R2 and R3 are the same or different and are hydrogen, halogen, alkyl of 1 to 4 carbons or cycloalkyl of 3 to 5 carbons, provided that at least one of R2 and R3 is other than hydrogen; R4 is R5 and R6 are the same or different and are selected from hydrogen, aryl, heteroaryl, alkyl, cycloalkyl, aralkyl or heteroaralkyl. R7 is aryl, heteroaryl, alkyl, aralkyl, or heteroaralkyl; R8 is aryl, heteroaryl, or cycloalkyl; R9 is R7 or hydrogen; R10 is hydrogen, halogen, cyano or alkyl; R11 and R12 are each independently selected from the group consisting of hydrogen, halogen, alkoxy, hydroxy (—OH) cyano, and alkyl; R13 is carboxylic acid (COOH) or esters thereof, phosphonic and phosphinic acid or esters thereof, sulfonic acid, tetrazole, hydroxamic acid, thiazolidinedione, acylsulfonamide, or other carboxylic acid surrogates known in the art; R14 and R15 may be the same or different and are selected from hydrogen and alkyl, or R14 and R15 may be joined together forming a chain of 2 to 5 methylene groups [—(CH2)m-, m=2, 3, 4 or 5], thus forming 3- to 6-membered cycloalkyl rings; R16 is hydrogen or alkyl of 1 to 4 carbons; R17 and R18 are the same or different and selected from hydrogen, halogen and alkyl; n is 0 or an integer from 1 to 4; X is oxygen (—O—), sulfur (—S—), sulfonyl (—SO2—), sulfenyl (—SO—) selenium (—Se—), carbonyl (—CO—), amino (—NH—) or methylene (—CH2-); wherein the substituents are as described herein. In addition, a method is provided for preventing, inhibiting or treating diseases or disorders associated with metabolism dysfunction or which are dependent upon the expression of a T3 regulated gene, wherein a compound as described above is administered in a therapeutically effective amount.
摘要翻译：提供具有通式I的甲状腺受体配体，其中：R 1是R 2和R 3相同或不同，是氢，卤素，1至4个碳的烷基或3至5个碳原子的环烷基，条件是R2中的至少一个并且R 3不是氢; R 4是R 5和R 6相同或不同，并且选自氢，芳基，杂芳基，烷基，环烷基，芳烷基或杂芳烷基。 R7是芳基，杂芳基，烷基，芳烷基或杂芳烷基; R8是芳基，杂芳基或环烷基; R9为R7或氢; R 10是氢，卤素，氰基或烷基; R 11和R 12各自独立地选自氢，卤素，烷氧基，羟基（-OH）氰基和烷基; R13是羧酸（COOH）或其酯，膦酸和次膦酸或其酯，磺酸，四唑，异羟肟酸，噻唑烷二酮，酰基磺酰胺或本领域已知的其它羧酸替代物; R 14和R 15可以相同或不同，并且选自氢和烷基，或者R 14和R 15可以连接在一起形成2至5个亚甲基 - [ - （CH 2）m - ，m = 2,3,4或 5]，从而形成3-至6-元环烷基环; R16是氢或1至4个碳的烷基; R 17和R 18相同或不同，选自氢，卤素和烷基; n为0或1至4的整数; X是氧（-O-），硫（-S-），磺酰基（-SO 2 - ），亚磺酰基（-SO-），硒（-Se-），羰基（-CO-），氨基（-NH-）或亚甲基（-CH2-）; 其中取代基如本文所述。此外，提供了一种用于预防，抑制或治疗与代谢功能障碍相关或依赖于T3调节基因的表达的疾病或病症的方法，其中如上所述的化合物以治疗有效量施用。

9. 发明授权

US06831102B2 Phenyl naphthol ligands for thyroid hormone receptor 失效
标题翻译：用于甲状腺激素受体的苯基萘酚配体
公开(公告)号：US06831102B2
公开(公告)日：2004-12-14
申请号：US10313864
申请日：2002-12-06
申请人： Jon J. Hangeland
发明人： Jon J. Hangeland
IPC分类号： A01N3710
CPC分类号： C07C233/56 , A61K31/195 , A61K31/198 , A61K45/06 , C07C59/56 , C07C229/18 , C07C233/25 , A61K2300/00
摘要： New thyroid receptor ligands are provided which have the general formula I: wherein R1 is halogen, trifluoromethyl, substituted or unsubstituted aryl, substituted or unsubstituted C1-6 alkyl, or substituted or unsubstituted C3-7 cycloalkyl; R2 and R3 are each independently hydrogen, halogen, substituted or unsubstituted C1-4 alkyl, or substituted or unsubstituted C3-6 cycloalkyl, wherein at least one of R2 and R3 is other than hydrogen; R4 is a carboxylic acid selected from the group consisting of (CH2)nCOOH, (CH)2COOH, NHCO(CH2)nCOOH, CONH(CH2)nCOOH and NH(CH2)mCOOH; n is an integer from 0 to 4; and m is an integer from 1 to 4. In addition, a method is provided for preventing, inhibiting or treating a disease associated with metabolism dysfunction or which is dependent upon the expression of a T3 regulated gene, wherein a compound as described above is administered in a therapeutically effective amount.
摘要翻译：提供了具有通式I的新型甲状腺受体配体：其中R1是卤素，三氟甲基，取代或未取代的芳基，取代或未取代的C1-6烷基或取代或未取代的C3-7环烷基; R2和R3各自独立地为氢，卤素取代或未取代的C 1-4烷基或取代或未取代的C 3-6环烷基，其中R 2和R 3中的至少一个不是氢; R 4是选自（CH 2）n COOH，（CH） 2COOH，NHCO（CH 2）n COOH，CONH（CH 2）n COOH和NH（CH 2）m COOH; n为0至4的整数; andm为1〜4的整数。另外，提供了用于预防，抑制或治疗与代谢功能障碍相关的疾病或依赖于T3调节基因的表达的方法，其中将上述化合物以治疗有效量。

10. 发明授权

US5994517A Ligands to enhance cellular uptake of biomolecules 失效
标题翻译：配体增强生物分子的细胞摄取
公开(公告)号：US5994517A
公开(公告)日：1999-11-30
申请号：US755062
申请日：1996-11-22
申请人： Paul O. P. Ts'o , Jon J. Hangeland , Yuan C. Lee
发明人： Paul O. P. Ts'o , Jon J. Hangeland , Yuan C. Lee
IPC分类号： A61K31/00 , A61K31/70 , A61K31/7088 , A61K31/7125 , A61K47/48 , A61K48/00 , A61P1/00 , A61P1/16 , C07H15/18 , C07H21/00 , C07K16/00
CPC分类号： C07H21/00 , A61K47/48092 , A61K47/48276 , C07H15/18
摘要： Oligodeoxynucleoside methylphosphonate neoglycopeptide conjugates and related compounds for tissue specific delivery of biologically stable, nonionic oligodeoxynucleoside analogs into cells.
摘要翻译：寡脱氧核苷甲基膦酸盐新聚糖共轭物和相关化合物，用于组织特异性递送生物稳定的非离子寡脱氧核苷类似物进入细胞。

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