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1. 发明申请

US20230139282A1 ANTIMALARIAL AGENTS 有权
公开(公告)号：US20230139282A1
公开(公告)日：2023-05-04
申请号：US17795349
申请日：2021-02-02
申请人： Manuel DE LERA RUIZ , Paola FAVUZZA , Zhuyan GUO , Bin HU , Michael J. KELLY, III , Zhiyu LEI , John A. MCCAULEY , David B. OLSEN , Brad SLEEBS , Tony TRIGLIA , Dongmei ZHAN , Lianyun ZHAO , Merck Sharp & Dohme LLC , The Walter and Eliza Hall Institute of Medical Research , MSD R&D (China) Co., Ltd.
发明人： Manuel de Lera Ruiz , Paola Favuzza , Zhuyan Guo , Bin Hu , Michael J. Kelly, III , Zhiyu Lei , John A. McCauley , David B. Olsen , Brad Sleebs , Tony Triglia , Dongmei Zhan , Lianyun Zhao
IPC分类号： A61K31/513 , A61K45/06 , C07D405/12 , C07D233/88 , C07D405/14 , C07D417/14 , C07D491/18 , A61P33/06 , A61K31/529 , A61K31/5377 , C07D401/06
摘要： Provided are methods of treating malaria comprising administration of compounds of Formula (I) or a pharmaceutically acceptable salt thereof, to a subject in need thereof, wherein the variables are as defined herein. Also provided are uses of the compounds of Formula (I), as defined herein, for treating a Plasmodium infection, and for treating malaria. Also provided are methods of treatment further comprising administration of one or more additional anti-malarial compounds.

2. 发明申请

US20230013692A1 ANTIMALARIAL AGENTS 有权
公开(公告)号：US20230013692A1
公开(公告)日：2023-01-19
申请号：US17776040
申请日：2020-11-16
申请人： Merck Sharp & Dohme LLC , MSD R&D (China) Co. Ltd. , The Walter and Eliza Hall Institute of Medical Research
发明人： John A. McCauley , Manuel de Lera Ruiz , Zhuyan Guo , Bin Hu , Michael J. Kelly, III , Zhiyu Lei , David B. Olsen , Brad Sleebs , Dongmei Zhan , Lianyun Zhao
IPC分类号： C07D239/22 , C07D401/06 , C07D405/14 , A61P33/06
摘要： The present invention provides methods of treating malaria comprising administration of compounds of Formula (I) or a pharmaceutically acceptable salt thereof, to a subject in need thereof, wherein the variables are as defined herein. The invention also provides uses of the compounds of Formula (I), as defined herein, for the possible inhibition of plasmepsin X, plasmepsin IX or plasmepsin X and IX activity, for treating a Plasmodium infection, and for treating malaria. Also provided are methods of treatment further comprising administration of one or more additional anti-malarial compounds.

3. 发明申请

US20220331321A1 ANTIMALARIAL AGENTS 有权
公开(公告)号：US20220331321A1
公开(公告)日：2022-10-20
申请号：US17633655
申请日：2020-07-21
申请人： Merck Sharp & Dohme Corp. , The Walter and Eliza Hall Institute of Medical Research , MSD R & D (China) Co. LTD.
发明人： John A. McCauley , Alan F. Cowman , Manuel de Lera Ruiz , Paola Favuzza , Zhuyan Guo , Bin Hu , Michael J. Kelly, III , Zhiyu Lei , David B. Olsen , Brad Sleebs , Jennifer K. Thompson , Tony Triglia , Dongmei Zhan , Cailing Zhang , Lianyun Zhao
IPC分类号： A61K31/513 , C07D405/14 , C07D493/10 , C07D491/052 , C07D409/14 , C07D239/22 , C07D405/12 , C07D409/04 , A61P33/06 , A61K45/06
摘要： Methods of treating malaria comprising administration of compounds of Formula (I′) or a pharmaceutically acceptable salt thereof, to a subject in need thereof, wherein the variables are as defined herein. It also provides uses of the compounds of Formula (I), as defined herein, for inhibiting plasmepsin X, plasmepsin IX or plasmepsin X and IX activity, for treating a Plasmodium infection, and for treating malaria. Also provided are methods of treatment further comprising administration of one or more additional anti-malarial compounds.

4. 发明申请

US20160214997A1 2,2-DIFLUORODIOXOLO A2A RECEPTOR ANTAGONISTS 审中-公开
标题翻译： 2,2-DIFLUORODIOXOLO A2A受体拮抗剂
公开(公告)号：US20160214997A1
公开(公告)日：2016-07-28
申请号：US14914843
申请日：2014-08-25
申请人： Amjad ALI , Gioconda V. GALLO , Timothy J. HENDERSON , Rongze KUANG , Yeon-Hee LIM , Michael Man-Chu LO , Edward METZGER , Manuel de Lera RUIZ , Andrew STAMFORD , Paul TEMPEST , Brent WHITEHEAD , Heping WU , MERCK SHARP & DOHME CORP.
发明人： Ali Amjad , Gioconda V. Gallo , Timothy J. Henderson , Rongze Kuang , Yeon-Hee Lim , Michael Man-Chu Lo , Edward Metzger , Manuel de Lera Ruiz , Andrew Stamford , Paul Tempest , Brent Whitehead , Heping Wu
IPC分类号： C07D519/00 , C07D491/147
CPC分类号： C07D519/00 , C07D491/147
摘要： The present invention is directed to 2,2-difluorodioxolo compounds that are antagonists of A2A receptor. The present invention is also directed to uses of the 2,2-difluorodioxolo compounds described herein in the potential treatment or prevention of neurological disorders and diseases in which A2A receptor are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds and to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which A2A receptors are involved.
摘要翻译：本发明涉及作为A2A受体拮抗剂的2,2-二氟二氧代己基化合物。本发明还涉及本文所述的2,2-二氟二氧代环戊基化合物在涉及A2A受体的神经障碍和疾病的潜在治疗或预防中的用途。本发明还涉及包含这些化合物的药物组合物以及这些药物组合物用于预防或治疗其中涉及A2A受体的疾病的用途。

5. 发明授权

US07879880B2 Substituted aniline derivatives useful as histamine H3 antagonists 失效
标题翻译：用作组胺H3拮抗剂的取代苯胺衍生物
公开(公告)号：US07879880B2
公开(公告)日：2011-02-01
申请号：US11641153
申请日：2006-12-19
申请人： Daniel M. Solomon , Robert G. Aslanian , Michael Y. Berlin , Manuel de Lera Ruiz , Kevin D. McCormick , Mwangi W. Mutahi , Wing C. Tom
发明人： Daniel M. Solomon , Robert G. Aslanian , Michael Y. Berlin , Manuel de Lera Ruiz , Kevin D. McCormick , Mwangi W. Mutahi , Wing C. Tom
IPC分类号： A61K31/5377 , A61K31/496 , A61K31/4545 , C07D487/04 , C07D413/14 , C07D401/14 , C07D401/12
CPC分类号： C07D401/12 , C07D213/73 , C07D213/74 , C07D401/14 , C07D471/04
摘要： Disclosed are compounds of the formula or a pharmaceutically acceptable salt thereof, wherein M1 is M2 is N; X is a bond, optionally substituted alkylene, alkenylene, —O—, —CH2N(R12)—, —N(R12)CH2—, —N(R12)—, —NHC(O)—, —OCH2—, —CH2O—, or —S(O)0-2—; and Y is —(CH2)1-2—, —C(═O)—, —C(═NOR13)— or —SO0-2—; or M1 is N; M2 is N or CH; X is a bond, alkylene, alkenylene, —C(O)—, —NHC(O)—, —OC(O)— or —S(O)1-2—; Y is —(CH2)1-2—, —C(═O)— or —SO0-2—; and when M2 is CH, Y is also Y is —O— or —C(═NOR13)—; Z is a bond or optionally substituted alkylene or alkenylene; U and W are CH, or one is CH and one is N; R1 is optionally substituted alkyl, cycloalkyl, aryl, arylalkyl, heteroaryl, heterocycloalkyl; R2 is optionally substituted alkyl, alkenyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl or heterocycloalkyl; and the remaining variables are as defined in the specification; and compositions and methods of treating obesity, metabolic syndrome and a cognition deficit disorder, alone or in combination with other agents.
摘要翻译：公开了下式的化合物或其药学上可接受的盐，其中M 1为M 2为N; X是一个键，任选取代的亚烷基，亚烯基，-O - ， - CH2-（R12） - ， - N（R12）CH2-，-N（R12） - ， - NHC（O） - ， - OCH2 - - 或-S（O）0-2-; 并且Y是 - （CH 2）1-2 - ， - C（= O） - ， - C（= NOR 13） - 或-SOO 2 - ; 或M1为N; M2为N或CH; X是键，亚烷基，亚烯基，-C（O） - ， - NHC（O） - ， - OC（O） - 或-S（O）1-2 - Y是 - （CH 2）1-2 - ， - C（= O） - 或-SOO 2 - ; 当M2是CH时，Y也是Y是-O-或-C（= NROR13） - ; Z是键或任选取代的亚烷基或亚烯基; U和W是CH，或一个是CH，一个是N; R 1是任选取代的烷基，环烷基，芳基，芳基烷基，杂芳基，杂环烷基; R 2是任选取代的烷基，烯基，芳基，芳基烷基，杂芳基，杂芳基烷基，环烷基或杂环烷基; 剩余的变量如规范中所定义; 以及单独或与其他药物组合治疗肥胖症，代谢综合征和认知缺陷障碍的组合物和方法。

6. 发明申请

US20080039439A1 Alpha2C adrenoreceptor agonists 失效
标题翻译： α2C肾上腺素受体激动剂
公开(公告)号：US20080039439A1
公开(公告)日：2008-02-14
申请号：US11705673
申请日：2007-02-13
申请人： Kevin McCormick , Christopher Boyce , Neng-Yang Shih , Chia-Yu Huang , Robert Aslanian , Salem Fevrier , Bo Liang , Rong-qiang Liu , Ruiyan Liu , Pietro Mangiaracina , Manuel de Lera Ruiz , Younong Yu , Lisa Guise-Zawacki , Junying Zheng
发明人： Kevin McCormick , Christopher Boyce , Neng-Yang Shih , Chia-Yu Huang , Robert Aslanian , Salem Fevrier , Bo Liang , Rong-qiang Liu , Ruiyan Liu , Pietro Mangiaracina , Manuel de Lera Ruiz , Younong Yu , Lisa Guise-Zawacki , Junying Zheng
IPC分类号： A61K31/535 , A61K31/502 , A61K31/54 , A61K31/553 , A61P1/00 , A61P25/00 , A61P37/00 , A61P9/00 , C07D241/36 , C07D279/06 , C07D498/04 , C12N5/06
CPC分类号： C07D413/14 , C07D241/36 , C07D279/06 , C07D403/06 , C07D413/06 , C07D417/06 , C07D417/14 , C07D471/04 , C07D498/04
摘要： In its many embodiments, the present invention relates to a novel class of phenylmorpholine and phenylthiomorpholine compounds useful as α2C adrenergic receptor agonists, pharmaceutical compositions containing the compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the α2C adrenergic receptor agonists using such compounds or pharmaceutical compositions.
摘要翻译：在其许多实施方案中，本发明涉及可用作α2C肾上腺素能受体激动剂的新型苯基吗啉和苯硫基吗啉化合物，含有该化合物的药物组合物，以及治疗，预防，抑制或改善一种或多种与 α2C肾上腺素能受体激动剂，使用这些化合物或药物组合物。

7. 发明申请

US20070066644A1 1-[[1-[(2-Amino-6-methyl-4-pyridinyl)methyl]-4-fluoro-4-piperidinyl]carbonyl]-4-[2-(2-pyridinyl)-3H-imidazo[4,5-b]pyridin-3-yl]piperidine 失效
标题翻译： 1 - [[1 - [（2-氨基-6-甲基-4-吡啶基）甲基] -4-氟-4-哌啶基]羰基] -4- [2-（2-吡啶基）-3H-咪唑并[4 ，5-b]吡啶-3-基]哌啶
公开(公告)号：US20070066644A1
公开(公告)日：2007-03-22
申请号：US11523489
申请日：2006-09-19
申请人： Manuel de Lera Ruiz , Robert Aslanian , Michael Berlin , Kevin McCormick , Chander Celly
发明人： Manuel de Lera Ruiz , Robert Aslanian , Michael Berlin , Kevin McCormick , Chander Celly
IPC分类号： A61K31/4745 , C07D471/02
CPC分类号： C07D471/04
摘要： The present invention discloses the compound of Formula I and pharmaceutically acceptable salts and solvates thereof. The invention also relates to pharmaceutical compositions comprising the Compound of Formula I and its use in treating obesity, metabolic syndrome, diabetes, hepatic lipidosis or nonalcoholic fatty liver disease. The invention also relates to the use of a combination of the Compound of Formula I with additional therapeutic agents for treating obesity, metabolic syndrome, diabetes, hepatic lipidosis or nonalcoholic fatty liver disease.
摘要翻译：本发明公开了式I化合物及其药学上可接受的盐和溶剂化物。本发明还涉及包含式I化合物及其在治疗肥胖，代谢综合征，糖尿病，肝脏脂质沉积或非酒精性脂肪性肝病中的用途的药物组合物。本发明还涉及式I化合物与用于治疗肥胖，代谢综合征，糖尿病，肝脏脂质沉积或非酒精性脂肪性肝病的其它治疗剂的组合的用途。

8. 发明申请

US20110251207A1 BIARYL-SPIROAMINOOXAZOLINE ANALOGUES AS ALPHA 2C ADRENERGIC RECEPTOR MODULATORS 失效
标题翻译：作为ALPHA 2C ADRENERGIC受体调节剂的BIARYL-SPIROAMINOOXAZOLINE ANALOGUES
公开(公告)号：US20110251207A1
公开(公告)日：2011-10-13
申请号：US13122679
申请日：2009-10-06
申请人： Kevin D. McCormick , Li Dong , Christopher W. Boyce , Manuel de Lera Ruiz , Salem Fevrier , Jie Wu , Junying Zheng , Younong Yu , Jianhua Chao , Walter S. Won , Ashwin U. Rao , Rongze Kuang , Pauline C. Ting , Xianhai Huang , Ning Shao , Adandan Palani , Michael Y. Berlin , Robert G. Aslanian
发明人： Kevin D. McCormick , Li Dong , Christopher W. Boyce , Manuel de Lera Ruiz , Salem Fevrier , Jie Wu , Junying Zheng , Younong Yu , Jianhua Chao , Walter S. Won , Ashwin U. Rao , Rongze Kuang , Pauline C. Ting , Xianhai Huang , Ning Shao , Adandan Palani , Michael Y. Berlin , Robert G. Aslanian
IPC分类号： A61K31/501 , A61K31/506 , A61K31/4439 , A61K31/427 , A61K31/497 , C07D263/52 , A61K31/423 , C07D235/02 , A61K31/4184 , C07D405/10 , C07D409/10 , A61K31/422 , C07D403/10 , A61P27/06 , A61P25/22 , A61P21/02 , A61P9/00 , A61P25/18 , A61P25/06 , A61P25/28 , A61P3/10 , A61P11/02 , C07D413/10
CPC分类号： A61K31/5377 , A61K31/437 , A61K31/501 , A61K31/506 , A61K31/537 , C07D235/02 , C07D263/52 , C07D401/10 , C07D403/10 , C07D405/10 , C07D409/10 , C07D413/10 , C07D413/14 , C07D417/10 , C07D471/04 , C07D498/10 , C07D519/00
摘要： In its many embodiments, the present invention provides a novel class of biaryi spiroaminooxazoline analogues as modulators of α2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the α2C adrenergic receptors using such compounds or pharmaceutical compositions.
摘要翻译：在其许多实施方案中，本发明提供了一类新颖的作为α2C肾上腺素能受体激动剂的调节剂的生物二螺吡喃恶唑啉类似物，制备这些化合物的方法，含有一种或多种这类化合物的药物组合物，制备包含一种或多种这类化合物的药物制剂的方法以及使用这些化合物或药物组合物治疗，预防，抑制或改善与α2C肾上腺素能受体相关的一种或多种病症的方法。

9. 发明授权

US07985748B2 ALPHA2C adrenoreceptor agonists 失效
标题翻译： ALPHA2C肾上腺素受体激动剂
公开(公告)号：US07985748B2
公开(公告)日：2011-07-26
申请号：US12722879
申请日：2010-03-12
申请人： Kevin D. McCormick , Christopher W. Boyce , Neng-Yang Shih , Robert G. Aslanian , Pietro Mangiaracina , Manuel de Lera Ruiz , Younong Yu , Purakkattle Biju , Chia-Yu Huang , Bo Liang , Ruiyan Liu , Rong-Qiang Liu , Lisa Guise-Zawacki
发明人： Kevin D. McCormick , Christopher W. Boyce , Neng-Yang Shih , Robert G. Aslanian , Pietro Mangiaracina , Manuel de Lera Ruiz , Younong Yu , Purakkattle Biju , Chia-Yu Huang , Bo Liang , Ruiyan Liu , Rong-Qiang Liu , Lisa Guise-Zawacki
IPC分类号： C07D413/06 , A61K31/538
CPC分类号： C07D413/06 , C07D403/06 , C07D413/04 , C07D413/14 , C07D417/06 , C07D471/04 , C07D487/04 , C07D498/04
摘要： In its many embodiments, the present invention relates to a novel class of phenylmorpholine and phenylthiomorpholine compounds useful as α2C adrenergic receptor agonists, pharmaceutical compositions containing the compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the α2C adrenergic receptor agonists using such compounds or pharmaceutical compositions.
摘要翻译：在其许多实施方案中，本发明涉及可用作α2C肾上腺素能受体激动剂的新一类苯基吗啉和苯硫基吗啉化合物，含有该化合物的药物组合物，以及治疗，预防，抑制或改善一种或多种与 α2C肾上腺素能受体激动剂，使用这些化合物或药物组合物。

10. 发明申请

US20070142394A1 Substituted aniline derivatives useful as histamine H3 antagonists 失效
标题翻译：用作组胺H3拮抗剂的取代苯胺衍生物
公开(公告)号：US20070142394A1
公开(公告)日：2007-06-21
申请号：US11641153
申请日：2006-12-19
申请人： Daniel Solomon , Robert Aslanian , Michael Berlin , Manuel de Lera Ruiz , Kevin McCormick , Mwangi Mutahi , Wing Tom
发明人： Daniel Solomon , Robert Aslanian , Michael Berlin , Manuel de Lera Ruiz , Kevin McCormick , Mwangi Mutahi , Wing Tom
IPC分类号： A61K31/496 , A61K31/4545 , C07D403/14 , C07D401/14
CPC分类号： C07D401/12 , C07D213/73 , C07D213/74 , C07D401/14 , C07D471/04
摘要： Disclosed are compounds of the formula or a pharmaceutically acceptable salt thereof, wherein M1 is M2 is N; X is a bond, optionally substituted alkylene, alkenylene, —O—, —CH2N(R12)—, —N(R12)CH2—, —N(R12)—, —NHC(O)—, —OCH2—, —CH2O—, or —S(O)0-2—; and Y is —(CH2)1-2—, —C(═O)—, —C(═NOR13)— or —SO0-2—; or M1 is N; M2 is N or CH; X is a bond, alkylene, alkenylene, —C(O)—, —NHC(O)—, —OC(O)— or —S(O)1-2—; Y is —(CH2)1-2—, —C(═O)— or —SO0-2—; and when M2 is CH, Y is also Y is —O— or —C(═NOR13)—; Z is a bond or optionally substituted alkylene or alkenylene; U and W are CH, or one is CH and one is N; R1 is optionally substituted alkyl, cycloalkyl, aryl, arylalkyl, heteroaryl, heterocycloalkyl; R2 is optionally substituted alkyl, alkenyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl or heterocycloalkyl; and the remaining variables are as defined in the specification; and compositions and methods of treating obesity, metabolic syndrome and a cognition deficit disorder, alone or in combination with other agents.
摘要翻译：公开了下式的化合物或其药学上可接受的盐，其中M 1是M 2是N; X是一个键，任选取代的亚烷基，亚烯基，-O - ， - CH 2 N（R 12） - ， - N（R 12） CH 2 - ， - N（R 12） - ， - NHC（O） - ， - OCH 2 - ， - O 2或-S（O）0-2 - ; 并且Y是 - （CH 2）2 - ， - C（ - ） - ， - C（-NOR 13） - 或-SO <0-2 < - >。或M 1是N; M 2是N或CH; X是键，亚烷基，亚烯基，-C（O） - ， - NHC（O） - ， - OC（O） - 或-S（O） Y是 - （CH 2）2 - ， - C - （ - O） - 或-SO 0-2 - 。当M 2是CH时，Y也是Y是-O-或-C（-NOR 13） - ; Z是键或任选取代的亚烷基或亚烯基; U和W是CH，或一个是CH，一个是N; R 1是任选取代的烷基，环烷基，芳基，芳烷基，杂芳基，杂环烷基; R 2是任选取代的烷基，烯基，芳基，芳基烷基，杂芳基，杂芳基烷基，环烷基或杂环烷基; 剩余的变量如规范中所定义; 以及单独或与其他药物组合治疗肥胖症，代谢综合征和认知缺陷障碍的组合物和方法。

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