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1. 发明授权

US09550750B2 Indoline compounds as aldosterone synthase inhibitors 有权
标题翻译：二氢吲哚化合物作为醛固酮合酶抑制剂
公开(公告)号：US09550750B2
公开(公告)日：2017-01-24
申请号：US14433441
申请日：2013-10-02
申请人： Merck Sharp & Dohme Corp. , ElexoPharm GmbH , Amjad Ali , Michael Man-Chu Lo , Edward Metzger , Lina Yin , Rolf Hartmann , Qingzhong Hu , Ralf Heim , Christina Zimmer
发明人： Amjad Ali , Michael Man-Chu Lo , Edward Metzger , Lina Yin , Rolf Hartmann , Qingzhong Hu , Ralf Heim , Christina Zimmer
IPC分类号： C07D401/04 , A61K31/4439 , A61K45/06 , A61K31/4709 , C07D409/14
CPC分类号： C07D401/04 , A61K31/4439 , A61K31/4709 , A61K31/4725 , A61K45/06 , C07D409/14 , A61K2300/00
摘要： This invention relates to indo line compounds of the structural formula I, or their pharmaceutically acceptable salts, wherein the variables are defined herein. The inventive compounds selectively inhibit aldosterone synthase. This invention also provides for pharmaceutical compositions comprising the compounds of Formula I or their salts as well as potentially to methods for the treatment amelioration or prevention of conditions that could be treated by inhibiting aldosterone synthase.
摘要翻译：本发明涉及结构式I的吲哚类化合物或其药学上可接受的盐，其中变量在本文中定义。本发明化合物选择性地抑制醛固酮合酶。本发明还提供包含式I化合物或其盐的药物组合物，以及潜在的治疗改善或预防可通过抑制醛固酮合酶治疗的病症的方法。

2. 发明申请

US20110306624A1 GLUCAGON RECEPTOR ANTAGONIST COMPOUNDS, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF USE 有权
标题翻译： GLUCAGON受体拮抗剂化合物，包含这些化合物的组合物和使用方法
公开(公告)号：US20110306624A1
公开(公告)日：2011-12-15
申请号：US13148809
申请日：2010-02-03
申请人： Songnian Lin , Xibin Liao , Edward Metzger , Emma R. Parmee , Sheryl D. Debenham
发明人： Songnian Lin , Xibin Liao , Edward Metzger , Emma R. Parmee , Sheryl D. Debenham
IPC分类号： A61K31/4035 , C07D215/08 , A61K31/47 , C07D209/08 , A61K31/404 , C07D401/10 , A61K31/4439 , C07D403/12 , A61K31/4155 , C07D403/10 , A61K31/506 , C07D217/06 , A61K31/472 , A61P3/10 , C07D209/44
CPC分类号： A61K31/40
摘要： Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.
摘要翻译：公开了胰高血糖素受体拮抗剂化合物。该化合物可用于治疗2型糖尿病及相关病症。还包括药物组合物和治疗方法。

3. 发明授权

US06399640B1 Arylthiazolidinedione and aryloxazolidinedione derivatives 失效
标题翻译：芳基噻唑烷二酮和芳基恶唑烷二酮衍生物
公开(公告)号：US06399640B1
公开(公告)日：2002-06-04
申请号：US09595802
申请日：2000-06-16
申请人： Soumya P. Sahoo , Conrad Santini , Julia K. Boueres , James V. Heck , Edward Metzger , Victoria K. Lombardo
发明人： Soumya P. Sahoo , Conrad Santini , Julia K. Boueres , James V. Heck , Edward Metzger , Victoria K. Lombardo
IPC分类号： A61K31421
CPC分类号： C07D277/34 , C07D417/12
摘要： Substituted 5-aryl-2,4-thiazolidinediones or 5-aryl-2,4-oxazolidinediones that also carry a second substituent in the 5-position of the heterocyclic ring are potent agonists of PPAR, and are therefore useful in the treatment, control or prevention of diabetes, hyperglycemia, hyperlipidemia (including hypercholesterolemia and hypertriglyceridemia), atherosclerosis, obesity, vascular restenosis, and other PPAR &agr;, &dgr; and/or &ggr; mediated diseases, disorders and conditions.
摘要翻译：在杂环的5位上也带有第二取代基的5-芳基-2,4-噻唑烷二酮或5-芳基-2,4-恶唑烷二酮是PPAR的有效激动剂，因此可用于治疗，控制或预防糖尿病，高血糖症，高脂血症（包括高胆固醇血症和高甘油三酯血症），动脉粥样硬化，肥胖症，血管再狭窄和其他PPARα，δ和/或γ介导的疾病，病症和病症。

4. 发明申请

US20150361098A1 HETEROBICYCLO-SUBSTITUTED [1,2,4]TRIAZOLO[1,5-C]QUINAZOLIN-5-AMINE COMPOUNDS WITH A2A ANTAGONIST PROPERTIES 有权
标题翻译：取代[1,2,4]三唑[1,5-C]喹唑啉-5-胺化合物与A2A拮抗剂性质
公开(公告)号：US20150361098A1
公开(公告)日：2015-12-17
申请号：US14655648
申请日：2013-12-20
申请人： Amjad ALI , Michael Man-Chu LO , Yeon-Hee LIM , Andrew STAMFORD , Rongze KUANG , Paul TEMPEST , Younong YU , Xianhai HUANG , Timothy J. HENDERSON , Jae-Hun KIM , Christopher BOYCE , Pauline TING , Junying ZHENG , Edward METZGER , Nicolas ZORN , Dong XIAO , Gloconda GALLO , Walter WON , Heping WU , MERCH SHARP & DOHME CORP.
发明人： Amjad Ali , Michael Man-Chu Lo , Yeon-Hee Lim , Andrew Stamford , Rongze Kuang , Paul Tempest , Younong Yu , Xianhai Huang , Timothy J. Henderson , Jae-Hun Kim , Christopher Boyce , Pauline Ting , Junying Zheng , Edward Metzger , Nicolas Zorn , Dong Xiao , Gioconda V. Gallo , Walter Won , Heping Wu , Qiaolin Deng
IPC分类号： C07D519/00 , C07D487/04
CPC分类号： C07D519/00 , C07D487/04
摘要： Disclosed are compounds of Formula G1 (structurally represented): where “RG3” “Rd1” to “Rd4”, “n”, “m”, “p”, “W”, “X”, “Y”, and “Z” are defined herein which compounds are antagonists of A2A receptor. Disclosed herein also are uses of the compounds described herein as antagonists of the A2a receptor in the potential treatment or prevention of neurological disorders and diseases in which A2A receptors are involved. Disclosed herein also are pharmaceutical compositions comprising these compounds and uses of these pharmaceutical compositions.
摘要翻译：公开了式G1（结构表示）的化合物：其中“RG3”“Rd1”至“Rd4”，“n”，“m”，“p”，“W”，“X”，“Y”和“Z “在本文中定义为哪些化合物是A2A受体的拮抗剂。本文还公开了本文所述的化合物作为A2a受体的拮抗剂的潜在治疗或预防涉及A2A受体的神经障碍和疾病的用途。本文还公开了包含这些化合物的药物组合物和这些药物组合物的用途。

5. 发明申请

US20130289003A1 DIAZENIUMDIOLATE HETEROCYCLIC DERIVATIVES 有权
标题翻译：二氮杂环戊烷杂环衍生物
公开(公告)号：US20130289003A1
公开(公告)日：2013-10-31
申请号：US13881929
申请日：2011-10-25
申请人： Amjad Ali , Michael Man-Chu Lo , Robert K. Baker , Zhiqiang Guo , Brent Whitehead , Timothy J. Henderson , Edward Metzger , Lin Yan , Shrenik K. Shah , James Dellureficio , Jun Wang
发明人： Amjad Ali , Michael Man-Chu Lo , Robert K. Baker , Zhiqiang Guo , Brent Whitehead , Timothy J. Henderson , Edward Metzger , Lin Yan , Shrenik K. Shah , James Dellureficio , Jun Wang
IPC分类号： C07D207/12 , C07D205/04 , C07D413/10 , C07D403/10 , C07D307/20 , C07D309/12 , C07D211/44 , C07D401/04
CPC分类号： C07D211/44 , A61K31/655 , C07D205/04 , C07D207/12 , C07D207/16 , C07D207/273 , C07D307/20 , C07D309/12 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/10 , C07D413/04 , C07D413/10 , C07D417/04
摘要： A compound having the structure: useful for treating hypertension, Pulmonary Arterial Hypertension (PAH), congestive heart failure, conditions resulting from excessive water retention, cardiovascular disease, diabetes, oxidative stress, endothelial dysfunction, cirrhosis, pre-eclampsia, osteoporosis or nephropathy.
摘要翻译：具有以下结构的化合物：用于治疗高血压，肺动脉高压（PAH），充血性心力衰竭，由过度保水引起的病症，心血管疾病，糖尿病，氧化应激，内皮功能障碍，肝硬化，先兆子痫，骨质疏松症或肾病。

6. 发明授权

US08324384B2 Glucagon receptor antagonist compounds, compositions containing such compounds and methods of use 有权
标题翻译：胰高血糖素受体拮抗剂化合物，含有这些化合物的组合物和使用方法
公开(公告)号：US08324384B2
公开(公告)日：2012-12-04
申请号：US13148809
申请日：2010-02-03
申请人： Songnian Lin , Xibin Liao , Edward Metzger , Emma R. Parmee , Sheryl D. Debenham
发明人： Songnian Lin , Xibin Liao , Edward Metzger , Emma R. Parmee , Sheryl D. Debenham
IPC分类号： C07D209/08 , C07D209/44 , C07D215/08 , C07D217/06 , C07D401/10 , C07D403/10 , C07D403/12
CPC分类号： A61K31/40
摘要： Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.
摘要翻译：公开了胰高血糖素受体拮抗剂化合物。该化合物可用于治疗2型糖尿病及相关病症。还包括药物组合物和治疗方法。

7. 发明授权

US09108920B2 Diazeniumdiolate heterocyclic derivatives 有权
标题翻译：二氮烯鎓二醇杂环衍生物
公开(公告)号：US09108920B2
公开(公告)日：2015-08-18
申请号：US13881929
申请日：2011-10-25
申请人： Amjad Ali , Michael Man-Chu Lo , Robert K. Baker , Zhiqiang Guo , Brent Whitehead , Timothy J. Henderson , Edward Metzger , Lin Yan , Shrenik K. Shah , James Dellureficio , Jun Wang
发明人： Amjad Ali , Michael Man-Chu Lo , Robert K. Baker , Zhiqiang Guo , Brent Whitehead , Timothy J. Henderson , Edward Metzger , Lin Yan , Shrenik K. Shah , James Dellureficio , Jun Wang
IPC分类号： A61K31/655 , C07D207/12 , C07D211/44 , C07D205/04 , C07D207/16 , C07D207/273 , C07D307/20 , C07D309/12 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/10 , C07D413/04 , C07D413/10 , C07D417/04
CPC分类号： C07D211/44 , A61K31/655 , C07D205/04 , C07D207/12 , C07D207/16 , C07D207/273 , C07D307/20 , C07D309/12 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/10 , C07D413/04 , C07D413/10 , C07D417/04
摘要： A compound having the structure: useful for treating hypertension, Pulmonary Arterial Hypertension (PAH), congestive heart failure, conditions resulting from excessive water retention, cardiovascular disease, diabetes, oxidative stress, endothelial dysfunction, cirrhosis, pre-eclampsia, osteoporosis or nephropathy.
摘要翻译：具有以下结构的化合物：用于治疗高血压，肺动脉高压（PAH），充血性心力衰竭，由过度保水引起的病症，心血管疾病，糖尿病，氧化应激，内皮功能障碍，肝硬化，先兆子痫，骨质疏松症或肾病。

8. 发明申请

US20130296278A1 Diazeniumdiolate Derivatives 审中-公开
标题翻译：二氮烯二硫代衍生物
公开(公告)号：US20130296278A1
公开(公告)日：2013-11-07
申请号：US13980442
申请日：2012-01-12
申请人： Amjad Ali , Michael Man-Chu Lo , Edward Metzger , Shrenik K. Shah , James Dellureficio
发明人： Amjad Ali , Michael Man-Chu Lo , Edward Metzger , Shrenik K. Shah , James Dellureficio
IPC分类号： C07C291/02
CPC分类号： C07C291/02 , A61K45/06 , C07C291/08
摘要： A compound having the structure (I) useful for treating hypertension, pulmonary arterial hypertension, congestive heart failure, conditions resulting from excessive water retention, cardiovascular disease, diabetes, oxidative stress, endothelial dysfunction, cirrhosis, pre-eclampsia, osteoporosis or nephropathy.
摘要翻译：具有结构（I）的化合物，其可用于治疗高血压，肺动脉高压，充血性心力衰竭，由过度保水引起的病症，心血管疾病，糖尿病，氧化应激，内皮功能障碍，肝硬化，先兆子痫，骨质疏松症或肾病。

9. 发明授权

US08436015B2 Glucagon receptor antagonist compounds, compositions containing such compounds and methods of use 有权
标题翻译：胰高血糖素受体拮抗剂化合物，含有这些化合物的组合物和使用方法
公开(公告)号：US08436015B2
公开(公告)日：2013-05-07
申请号：US13063820
申请日：2009-09-10
申请人： Songnian Lin , Christian P. Stevenson , Emma R. Parmee , Libo Xu , Xibin Liao , Edward Metzger , Rui Liang , Fengqi Zhang , John E. Stelmach
发明人： Songnian Lin , Christian P. Stevenson , Emma R. Parmee , Libo Xu , Xibin Liao , Edward Metzger , Rui Liang , Fengqi Zhang , John E. Stelmach
IPC分类号： A01N43/42 , A61K31/47 , C07D215/00
CPC分类号： C07D215/18 , C07D215/227 , C07D217/22 , C07D217/24 , C07D239/70 , C07D403/04 , C07D413/04
摘要： Glucagon receptor antagonist compounds of formula I are disclosed: The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.
摘要翻译：公开了式I的胰高血糖素受体拮抗剂化合物：该化合物可用于治疗2型糖尿病和相关病症。还包括药物组合物和治疗方法。

10. 发明申请

US20130053352A1 DIAZENIUMDIOLATE CYCLOPENTYL DERIVATIVES 有权
标题翻译：二氮杂环戊烷衍生物
公开(公告)号：US20130053352A1
公开(公告)日：2013-02-28
申请号：US13577797
申请日：2011-02-10
申请人： Amjad Ali , Michael Man-Chu Lo , Edward Metzger , Lin Yan
发明人： Amjad Ali , Michael Man-Chu Lo , Edward Metzger , Lin Yan
IPC分类号： A61K31/655 , A61P9/12 , C07D249/04 , C07C245/24
CPC分类号： C07C291/00 , C07C291/08 , C07C2601/08 , C07D249/04
摘要： A compound having the structure or a pharmaceutically acceptable salt thereof, wherein R1 is hydrogen, —OH, —O—C1-6 alkyl, ═O, or halogen; R2 is hydrogen, C(O)OR8, C6H5C(O)OR8, (CH2)1-2OH, CR9R10OH, C(O)O(CH2)0-2 aryl, C(O)NR9R10, C(O)SO2NR9R10, C6H5OR9, W—C(O)OR8, W—OR9, Y, or P(O)(OR9)(ORlO); R3 is hydrogen or —C1-6 alkyl; R4 is hydrogen, —OH or —C(O)OR9; R5 is hydrogen or deuterium; R6 and R7 are independently —C1-6 alkyl, fluoro-substituted —C1-6 alkyl, deutero-substituted —C1-6 alkyl or —(CH2)1-2R11, wherein any carbon atom of the fluoro-substituted —C1-6 alkyl is mono- or di-substituted with fluoro, and any carbon atom of the deutero-substituted —C1-6 alkyl is mono- or di-substituted with fluoro; R8, in each instance in which it occurs, is independently hydrogen, —C1-6 alkyl, or —(CH2)2N+(CH3)3; R9 and R10, in each instance in which they occur, are independently —C1-6 alkyl; R11 is —OH, —O—C1-6 alkyl, -0CD3, —OC(O)OC1-6 alkyl, —NH2, —C6H5, —N3, or W; W is an unsubslituted 5- or 6-raembered heteroaryl ring having 1, 2, or 3 nitrogen atoms, or a substituted 5- or 6-membered heteroaryl ring having 1, 2, or 3 nitrogen atoms that is mono- or di-substituted at any carbon atom with R6 or R7; Y is a 5- or 6-membered heterocyclic ring having 1, 2, 3 or 4 heteroatoms which are N, O, or S or stereoisomers thereof, or pharmaceutically acceptable salts thereof, or pharmaceutically acceptable salts of stereoisomers thereof, and methods of using the compounds for treating hypertension.
摘要翻译：具有结构或其药学上可接受的盐的化合物，其中R 1是氢，-OH，-O-C 1-6烷基，= O或卤素; R2是氢，C（O）OR8，C6H5C（O）OR8，（CH2）1-2OH，CR9R10OH，C（O）O（CH2）O2芳基，C（O）NR9R10，C（O）SO2NR9R10， C6H5OR9，W-C（O）OR8，W-OR9，Y或P（O）（OR9）（OR10）。 R3是氢或-C 1-6烷基; R4是氢，-OH或-C（O）OR9; R5是氢或氘; R 6和R 7独立地是C 1-6烷基，氟取代的C 1-6烷基，取代的C 1-6烷基或 - （CH 2）1-2 R 11，其中氟取代的-C 1-6的任何碳原子烷基被氟单取代或二取代，氘取代的C 1-6烷基的任何碳原子被氟单取代或二取代; 在其每次发生的情况下，R 8独立地为氢，-C 1-6烷基或 - （CH 2）2 N +（CH 3）3; 在其各自出现的情况下，R 9和R 10独立地为-C 1-6烷基; R 11是-OH，-O-C 1-6烷基，-CD 3，-OC（O）OC 1-6烷基，-NH 2，-C 6 H 5，-N 3或W; W是具有1,2或3个氮原子的未取代的5-或6-元杂芳基环，或具有1,2或3个氮原子的取代的5-或6-元杂芳基环，其被单取代或二取代在任何具有R6或R7的碳原子上; Y是具有1,2,3或4个杂原子的5或6元杂环，其为N，O或S或其立体异构体，或其药学上可接受的盐，或其立体异构体的药学上可接受的盐，以及使用用于治疗高血压的化合物。

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