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1. 发明申请

US20040101523A1 Renal-selective prodrugs for control of renal smpathetic nerve activity in the treatment of hypertension 审中-公开
标题翻译：肾脏选择性前药用于控制治疗高血压的肾痉挛神经活动
公开(公告)号：US20040101523A1
公开(公告)日：2004-05-27
申请号：US10689919
申请日：2003-10-20
申请人： G.D. Searle & Co.
发明人： David B. Reitz , John P. Koepke , Edward H. Blaine , Joseph R. Schuh , Robert E. Manning , Glenn J. Smits
IPC分类号： A61K038/43 , C12N009/99
CPC分类号： C07D213/73 , C07C59/64 , C07C59/90 , C07C237/12 , C07C237/22 , C07D209/08 , C07D209/20 , C07D209/34 , C07D213/50 , C07D213/65 , C07D213/80 , C07D213/81 , C07D213/86 , C07D215/227 , C07D233/64 , C07D233/88 , C07D233/90 , C07D235/30 , C07D241/42 , C07D241/44 , C07D263/58 , C07D265/36 , C07D285/14 , C07D307/46 , C07D307/52 , C07D333/20 , C07D333/22 , C07D333/66
摘要： Renal-selective prodrugs are described which are preferentially converted in the kidney to compounds capable of inhibiting synthesis of catecholamine-type neurotransmitters involved in renal sympathetic nerve activity. The prodrugs described herein are derived from inhibitor compounds capable of inhibiting one or more of the enzymes involved in catecholamine synthesis, such compounds being classifiable as tyrosine hydroxylase inhibitors, or as dopa-decarboxylase inhibitors, or as dopamine-null-hydroxylase inhibitors. These inhibitor compounds are linked to a chemical moiety, such as a glutamic acid derivative, by a cleavable bond which is recognized selectively by enzymes located predominantly in the kidney. The liberated inhibitor compound is then available in the kidney to inhibit one or more of the enzymes involved in catecholamine synthesis. Inhibition of renal catecholamine synthesis can suppress heightened renal nerve activity associated with sodium-retention related disorders such as hypertension. Conjugates of particular interest are glutamyl derivatives of dopamine-null-hydroxylase inhibitors, of which N-acetyl-null-glutamyl fusaric acid hydrazide (shown below) is preferred. 1
摘要翻译：描述了肾选择性前药，其优先在肾中转化成能够抑制参与肾交感神经活性的儿茶酚胺型神经递质合成的化合物。本文所述的前药衍生自能够抑制一种或多种参与儿茶酚胺合成的酶的抑制剂化合物，这些化合物可分类为酪氨酸羟化酶抑制剂，或作为多巴 - 脱羧酶抑制剂，或作为多巴胺-β-羟化酶抑制剂。这些抑制剂化合物通过由主要位于肾中的酶选择性识别的可切割键与化学部分如谷氨酸衍生物连接。释放的抑制剂化合物然后可用于肾脏中以抑制参与儿茶酚胺合成的一种或多种酶。抑制肾脏儿茶酚胺合成可以抑制与钠滞留相关的疾病如高血压相关的增强的肾神经活动。特别感兴趣的缀合物是多巴胺-β-羟化酶抑制剂的谷氨酰衍生物，其中N-乙酰基-γ-谷氨酰镰孢酸酰肼（如下所示）是优选的。

2. 发明申请

US20030153602A1 3,4-diaryl thiophenes and analogs thereof having use as antiinflammatory agents 失效
标题翻译：具有用作抗炎剂的3,4-二芳基噻吩及其类似物
公开(公告)号：US20030153602A1
公开(公告)日：2003-08-14
申请号：US10329332
申请日：2002-12-27
申请人： G.D. Searle & Co.
发明人： John J. Talley , Stephen R. Bertenshaw , Paul W. Collins , Thomas D. Penning , David B. Reitz , Roland S. Rogers
IPC分类号： A61K031/4436 , A61K031/40 , A61K031/381 , A61K031/34
CPC分类号： C07D307/38 , A61K31/341 , A61K31/365 , C07D307/58 , C07D333/16 , C07D333/18 , C07D333/28 , C07D333/38 , C07D409/04
摘要： A class of 3,4-diaryl substituted thiophene, furan and pyrrole derivatives and analogs thereof, pharmaceutical compositions containing them and methods of using them to treat inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula I: 1 wherein Y is selected from O, S and NR1; wherein R1 is selected from hydrido and lower alkyl; wherein X is one or two substituent selected from hydrido, halo, lower alkoxycarbonyl and carboxyl; wherein R2 and R3 are independently aryl or heteroaryl; and wherein R2 and R3 are optionally substituted at a substitutable position with one or more radicals selected from sulfamyl, alkylsulfonyl, halo, lower alkoxy and lower alkyl; or a pharmaceutically-acceptable salt thereof.
摘要翻译：一类3,4-二芳基取代的噻吩，呋喃和吡咯衍生物及其类似物，含有它们的药物组合物和使用它们治疗炎症和炎症相关疾病的方法。特别感兴趣的化合物由式I定义：其中Y选自O，S和NR1; 其中R1选自氢和低级烷基; 其中X是一个或两个选自氢，卤素，低级烷氧基羰基和羧基的取代基; 其中R2和R3独立地是芳基或杂芳基; 并且其中R2和R3任选在可取代的位置被一个或多个选自磺酰胺基，烷基磺酰基，卤素，低级烷氧基和低级烷基的基团取代; 或其药学上可接受的盐。

3. 发明申请

US20020169206A1 Substituted biphenyl compounds for the treatment of inflammation 失效
标题翻译：用于治疗炎症的取代联苯化合物
公开(公告)号：US20020169206A1
公开(公告)日：2002-11-14
申请号：US09772595
申请日：2001-01-30
申请人： G.D. Searle & Co.
发明人： David B. Reitz , James J. Li , Monica B. Norton
IPC分类号： A61K031/277 , A61K031/36 , A61K031/135 , A61K031/10
CPC分类号： A61K31/277 , A61K31/10 , A61K31/135 , A61K31/36 , A61K31/44 , C07C311/16 , C07C311/29 , C07C311/39 , C07C317/14 , C07C317/22 , C07C317/32 , C07D213/34 , C07D317/56 , C07D319/18
摘要： A class of substituted biphenyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula III: 1 wherein each of R11 through R13 is independently selected from hydrido, halo, lower alkoxy, lower haloalkyl, amino, lower alkylamino, lower dialkylamino, and lower haloalkoxy; or wherein R11 and R12 together form nullO(CH2)nOnull; wherein n is 1-2, inclusive; or a pharmaceutically-acceptable salt thereof.
摘要翻译：描述了一类取代的联苯化合物用于治疗炎症和炎症相关疾病。特别感兴趣的化合物由式III定义：其中R11至R13各自独立地选自氢，卤素，低级烷氧基，低级卤代烷基，氨基，低级烷基氨基，低级二烷基氨基和低级卤代烷氧基; 或其中R 11和R 12一起形成-O（CH 2）n O-; 其中n为1-2; 或其药学上可接受的盐。

4. 发明申请

US20010020100A1 N-substituted-1, 2, 4-triazolone compounds for treatment of cardiovascular disorders 审中-公开
标题翻译：用于治疗心血管疾病的N-取代-1,2,4-三唑酮化合物
公开(公告)号：US20010020100A1
公开(公告)日：2001-09-06
申请号：US09742818
申请日：2000-12-20
申请人： G.D. Searle & Co.
发明人： Robert E. Manning , David B. Reitz , Horn-Chih Huang
IPC分类号： C07D249/12
CPC分类号： C07D403/10 , C07D249/12
摘要： A class of N-substituted-1,2,4-triazolone compounds is described for use in treatment of cardiovascular disorders. Compounds of particular interest are angiotensin II antagonists of the formula 1 wherein R1 is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, 4-methylbutyl, n-pentyl, neopentyl, phenyl, benzyl, phenethyl, cyclohexyl, cyclohexylmethyl, 1-oxoethyl, 1-oxopropyl, 1-oxobutyl, 1-oxopentyl and hydroxyalkyl; wherein R2 is selected from ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, 4-methylbutyl, tert-butyl, n-pentyl, neo-pentyl, propylthio and butylthio; wherein each of R3 through R11 is hydrido with the proviso that at least one of R5 and R9 must be selected from COOH, SH, PO3H2, SO3H, CONHNH2, CONHNHSO2CF3, OH, 2 wherein each of R42 and R43 is independently selected from chloro, cyano, nitro, trifluoromethyl, methoxycarbonyl and trifluoromethylsulfonyl. These compounds are particularly useful in treatment or control of hypertension and congestive heart failure.
摘要翻译：描述了一类用于治疗心血管疾病的N-取代的1,2,4-三唑酮化合物。特别感兴趣的化合物是下式的血管紧张素II拮抗剂，其中R1选自甲基，乙基，正丙基，异丙基，正丁基，仲丁基，异丁基，叔丁基，4-甲基丁基，正戊基，新戊基，苯基，苄基，苯乙基，环己基，环己基甲基，1-氧代乙基，1-氧代丙基，1-氧代丁基，1-氧代戊基和羟烷基; 其中R2选自乙基，正丙基，异丙基，正丁基，仲丁基，异丁基，4-甲基丁基，叔丁基，正戊基，新戊基，丙硫基和丁硫基; 其中R 3至R 11中的每一个是氢的，条件是R 5和R 9中的至少一个必须选自COOH，SH，PO 3 H 2，SO 3 H，CONHNH 2，CONHNHSO 2 CF 3，OH，其中R 42和R 43各自独立地选自氯，氰基，硝基，三氟甲基，甲氧基羰基和三氟甲基磺酰基。这些化合物特别可用于治疗或控制高血压和充血性心力衰竭。

5. 发明申请

US20040220245A1 Renal-selective biphenylalkyl 1H-substituted-1, 2, 4- triazole angiotensin I I antagonists for treatment of hypertension 失效
标题翻译：用于治疗高血压的肾选择性联苯基烷基1H-取代-1,4-三唑血管紧张素I 1拮抗剂
公开(公告)号：US20040220245A1
公开(公告)日：2004-11-04
申请号：US10852711
申请日：2004-05-24
申请人： G.D. Searle & Co.,
发明人： David B. Reitz , Robert E. Manning
IPC分类号： A61K031/4196
CPC分类号： C07D249/08 , C07D231/12 , C07D233/56 , C07D249/10 , C07D403/10 , H01M2/1055 , H04B1/3883 , H04B2001/3894
摘要： Renal-selective compounds are described which, in one embodiment, are prodrugs preferentially converted in the kidney to compounds capable of blocking angiotensin II (AII) receptors. These prodrugs are conjugates formed from two components, namely, a first component provided by an AII antagonist compound and a second component which is capable of being cleaved from the first component when both components are chemically linked within the conjugate. The two components are chemically linked by a bond which is cleaved selectively in the kidney, for example, by an enzyme. The liberated AII antagonist compound is then available to block AII receptors within the kidney. Conjugates of particular interest are glutamyl derivatives of biphenylmethyl 1H-substituted-1,2,4-triazole compounds, of which N-acetylglutamic acid, 5-nullnull4null-null(3,5-dibutyl-1H-1,2,4-triazol-1-yl)methylnullnull1,1null-biphenylnull-2-ylnullnullcarbonylhydrazide, (shown below) is an example: 1
摘要翻译：描述了肾选择性化合物，其在一个实施方案中是优先在肾中转化为能够阻断血管紧张素II（AII）受体的化合物的前药。这些前药是由两种组分形成的缀合物，即由AII拮抗剂化合物提供的第一组分和当两种组分在缀合物内化学连接时能够从第一组分切割的第二组分。两种组分通过在肾脏中有选择性地切割的键化学连接，例如通过酶。然后释放的AII拮抗剂化合物可用于阻断肾脏内的AII受体。特别感兴趣的结合物是联苯甲基1H-取代-1,2,4-三唑化合物的谷氨酰基衍生物，其中N-乙酰谷氨酸5 - [[4' - [（3,5-二丁基-1H-1,2,4-三唑） 4-三唑-1-基）甲基] [1,1'-联苯] -2-基]]羰酰肼，（如下所示）是一个实例：

6. 发明申请

US20040158074A1 Substituted biphenyl compounds for the treatment of inflammation 审中-公开
标题翻译：用于治疗炎症的取代联苯化合物
公开(公告)号：US20040158074A1
公开(公告)日：2004-08-12
申请号：US10756873
申请日：2004-01-13
申请人： G.D. Searle & Co.
发明人： David B. Reitz , James J. Li , Monica B. Norton
IPC分类号： C07D207/34 , C07C323/29
CPC分类号： A61K31/277 , A61K31/10 , A61K31/135 , A61K31/36 , A61K31/44 , C07C311/16 , C07C311/29 , C07C311/39 , C07C317/14 , C07C317/22 , C07C317/32 , C07D213/34 , C07D317/56 , C07D319/18
摘要： A class of substituted biphenyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula III: 1 wherein each of R11 through R13 is independently selected from hydrido, halo, lower alkoxy, lower haloalkyl, amino, lower alkylamino, lower dialkylamino, and lower haloalkoxy; or wherein R11 and R12 together form nullO(CH2)nOnull; wherein n is 1-2, inclusive; or a pharmaceutically-acceptable salt thereof.
摘要翻译：描述了一类取代的联苯化合物用于治疗炎症和炎症相关疾病。特别感兴趣的化合物由式III定义：其中R 11至R 13各自独立地选自氢，卤素，低级烷氧基，低级卤代烷基，氨基，低级烷基氨基，低级二烷基氨基和低级卤代烷氧基; 或其中R 11和R 12一起形成-O（CH 2）n O-; 其中n为1-2; 或其药学上可接受的盐。

7. 发明申请

US20040121989A1 Renal-selective biphenylalkyl 1H-substituted-1,2,4-triazole angiotensin II antagonists for treatment of hypertension 审中-公开
标题翻译：用于治疗高血压的肾选择性联苯基烷基1H-取代-1,2,4-三唑血管紧张素II拮抗剂
公开(公告)号：US20040121989A1
公开(公告)日：2004-06-24
申请号：US10326942
申请日：2002-12-19
申请人： G.D. Searle & Co.
发明人： David B. Reitz , Robert E. Manning
IPC分类号： A61K031/675 , A61K031/4196 , C07D263/36
CPC分类号： C07D249/08 , C07D231/12 , C07D233/56 , C07D249/10 , C07D403/10 , H01M2/1055 , H04B1/3883 , H04B2001/3894
摘要： Renal-selective compounds are described which, in one embodiment, are prodrugs preferentially converted in the kidney to compounds capable of blocking angiotensin II (AII) receptors. These prodrugs are conjugates formed from two components, namely, a first component provided by an AII antagonist compound and a second component which is capable of being cleaved from the first component when both components are chemically linked within the conjugate. The two components are chemically linked by a bond which is cleaved selectively in the kidney, for example, by an enzyme. The liberated AII antagonist compound is then available to block AII receptors within the kidney. Conjugates of particular interest are glutamyl derivatives of biphenylmethyl 1H-substituted-1,2,4-triazole compounds, of which N-acetylglutamic acid, 5-nullnull4null-null(3,5-dibutyl-1H-1,2,4-triazol-1-yl)methylnullnull1,1null-biphenylnull-2-ylnullnullcarbonylhydrazide, (shown below) is an example: 1
摘要翻译：描述了肾选择性化合物，其在一个实施方案中是优先在肾中转化为能够阻断血管紧张素II（AII）受体的化合物的前药。这些前药是由两种组分形成的缀合物，即由AII拮抗剂化合物提供的第一组分和当两种组分在缀合物内化学连接时能够从第一组分切割的第二组分。两种组分通过在肾脏中有选择性地切割的键化学连接，例如通过酶。然后释放的AII拮抗剂化合物可用于阻断肾脏内的AII受体。特别感兴趣的结合物是联苯甲基1H-取代-1,2,4-三唑化合物的谷氨酰基衍生物，其中N-乙酰谷氨酸5 - [[4' - [（3,5-二丁基-1H-1,2,4-三唑） 4-三唑-1-基）甲基] [1,1'-联苯] -2-基]]羰酰肼，（如下所示）是一个实例：

8. 发明申请

US20020013476A1 Novel benzothiepines having activity as inhibitors of ileal bile acid transport and taurocholate uptake 失效
标题翻译：具有作为回肠胆汁酸转运抑制剂和牛磺胆酸摄取的活性的新型苯并噻吖啶
公开(公告)号：US20020013476A1
公开(公告)日：2002-01-31
申请号：US09828968
申请日：2001-04-09
申请人： G.D. Searle & Co.
发明人： Len F. Lee , Shyamal C. Banerjee , Horng-Chih Huang , Jinglin J. Li , Raymond E. Miller , David B. Reitz , Samuel J. Tremont
IPC分类号： C07D337/08 , C07F009/547
CPC分类号： A61K31/38 , B24B5/18 , B24B21/12 , C07C319/14 , C07D337/06 , C07D337/08 , C07D409/10 , C07D409/12 , C07D487/08 , C07D495/04 , C07D495/10 , C07F9/65539 , C07K5/06086 , C08G65/329 , C07C323/12 , C07C323/18
摘要： Provided are novel benzothiepines, derivatives, and analogs thereof; pharmaceutical compositions containing them; and methods of using these compounds and compositions in medicine, particularly in the prophylaxis and treatment of hyperlipidemic conditions such as those associated with atherosclerosis or hypercholesterolemia, in mammals.
摘要翻译：提供了新的苯并噻庚因，衍生物和类似物; 含有它们的药物组合物; 以及在医学中使用这些化合物和组合物的方法，特别是用于预防和治疗哺乳动物中高脂血症的疾病，例如与动脉粥样硬化或高胆固醇血症有关的那些。

9. 发明申请

US20040014803A1 Novel benzothiepines having activity as inhibitors of lleal bile acid transport and taurocholate uptake 失效
标题翻译：具有作为胆汁酸运输抑制剂和牛磺胆酸摄取的活性的新型苯并噻庚英
公开(公告)号：US20040014803A1
公开(公告)日：2004-01-22
申请号：US10068297
申请日：2002-02-08
申请人： G.D. Searle & Co.
发明人： Len F. Lee , Shyamal C. Banerjee , Horng-Chih Huang , Jinglin J. Li , Raymond E. Miller , David B. Reitz , Samuel J. Tremont
IPC分类号： C07D337/16 , A61K031/38
CPC分类号： A61K31/38 , B24B5/18 , B24B21/12 , C07C319/14 , C07D337/06 , C07D337/08 , C07D409/10 , C07D409/12 , C07D487/08 , C07D495/04 , C07D495/10 , C07F9/65539 , C07K5/06086 , C08G65/329 , C07C323/12 , C07C323/18
摘要： Provided are novel benzothiepines, derivatives, and analogs thereof; pharmaceutical compositions containing them; and methods of using these compounds and compositions in medicine, particularly in the prophylaxis and treatment of hyperlipidemic conditions such as those associated with atherosclerosis or hypercholesterolemia, in mammals.
摘要翻译：提供了新的苯并噻庚因，衍生物和类似物; 含有它们的药物组合物; 以及在医学中使用这些化合物和组合物的方法，特别是用于预防和治疗哺乳动物中高脂血症的疾病，例如与动脉粥样硬化或高胆固醇血症有关的那些。

10. 发明申请

US20030013744A1 3,4-diaryl thiophenes and analogs thereof having use as anti-inflammatory agents 审中-公开
标题翻译：具有用作抗炎剂的3,4-二芳基噻吩及其类似物
公开(公告)号：US20030013744A1
公开(公告)日：2003-01-16
申请号：US10184960
申请日：2002-07-01
申请人： G.D. Searle & Co.
发明人： John J. Talley , Stephen R. Bertenshaw , Paul W. Collins , Thomas D. Penning , David B. Reitz , Roland S. Rogers
IPC分类号： C07D49/02 , C07D47/02 , C07D43/02 , A61K031/4436 , A61K031/4433 , A61K031/4025
CPC分类号： C07D307/38 , A61K31/341 , A61K31/365 , C07D307/58 , C07D333/16 , C07D333/18 , C07D333/28 , C07D333/38 , C07D409/04
摘要： A class of 3,4-diaryl substituted thiophene, furan and pyrrole derivatives and analogs thereof, pharmaceutical compositions containing them and methods of using them to treat inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula I: 1 wherein Y is selected from O, S and NR1; wherein R1 is selected from hydrido and lower alkyl; wherein X is one or two substituent selected from hydrido, halo, lower alkoxycarbonyl and carboxyl; wherein R2 and R3 are independently aryl or heteroaryl; and wherein R2 and R3 are optionally substituted at a substitutable position with one or more radicals selected from sulfamyl, alkylsulfonyl, halo, lower alkoxy and lower alkyl; or a pharmaceutically-acceptable salt thereof.
摘要翻译：一类3,4-二芳基取代的噻吩，呋喃和吡咯衍生物及其类似物，含有它们的药物组合物和使用它们治疗炎症和炎症相关疾病的方法。特别感兴趣的化合物由式I定义：其中Y选自O，S和NR1; 其中R1选自氢和低级烷基; 其中X是一个或两个选自氢，卤素，低级烷氧基羰基和羧基的取代基; 其中R2和R3独立地是芳基或杂芳基; 并且其中R2和R3任选在可取代的位置被一个或多个选自亚磺酰基，烷基磺酰基，卤素，低级烷氧基和低级烷基的基团取代; 或其药学上可接受的盐。

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