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1. 发明专利

JP2014051529A Pyridazinone derivative useful as glucan synthase inhibitor 审中-公开
标题翻译：吡咯烷酮衍生物作为GLUCAN SYNTHASE抑制剂有用
公开(公告)号：JP2014051529A
公开(公告)日：2014-03-20
申请号：JP2013259117
申请日：2013-12-16
申请人： Merck Sharp & Dohme Corp , メルク・シャープ・アンド・ドーム・コーポレーションMerck Sharp & Dohme Corp. , Albany Molecular Research Inc , アルバニーモレキュラーリサーチ, インコーポレイテッド
发明人： TING PAULINE C , ASLANIAN ROBERT G , CAO JIANHUA , KIM DAVID WON-SHIK , KUANG RONGZE , ZHOU GANG , HERR ROBERT JASON , ZYCH ANDREW JOHN , YANG JINHAI , WU HEPING , ZORN NICOLAS
IPC分类号： C07D237/22 , A61K31/501 , A61K31/5025 , A61K31/506 , A61K31/5355 , A61K31/536 , A61K31/541 , A61K31/664 , A61K31/695 , A61K31/706 , A61P31/10 , A61P43/00 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/04 , C07D471/10 , C07D487/04 , C07D487/08 , C07D487/14 , C07D513/04 , C07D515/18 , C07H15/203 , C12N9/99
CPC分类号： C07D401/14 , C07D403/04 , C07D403/14 , C07D407/14 , C07D409/14 , C07D413/14 , C07D487/08 , C07D515/22
摘要： PROBLEM TO BE SOLVED: To provide a pyridazinone derivative useful as a glucan synthase inhibitor.SOLUTION: In its many embodiments, the present invention provides: a substituted pyridazinone compound as a glucan synthase inhibitor; a method of preparing such a compound; a pharmaceutical including one or more of such a compound; a method of preparing pharmaceutical formulations including one or more of such a compound or one or more of such a compound along with another antifungal agent; and a method of treatment, prevention, inhibition, or amelioration of one or more fungal infections associated with glucan synthase using such a compound or a pharmaceutical composition.
摘要翻译：要解决的问题：提供可用作葡聚糖合酶抑制剂的哒嗪酮衍生物。解决方案：在其许多实施方案中，本发明提供：作为葡聚糖合酶抑制剂的取代的哒嗪酮化合物; 制备这种化合物的方法; 包括一种或多种这样的化合物的药物; 制备药物制剂的方法，包括一种或多种这样的化合物或一种或多种这样的化合物以及另一种抗真菌剂; 以及使用这种化合物或药物组合物治疗，预防，抑制或改善与葡聚糖合酶相关的一种或多种真菌感染的方法。

2. 发明专利

JP2013014622A Pyridazinone derivative useful as glucan synthase inhibitor 审中-公开
标题翻译：吡咯烷酮衍生物作为GLUCAN SYNTHASE抑制剂有用
公开(公告)号：JP2013014622A
公开(公告)日：2013-01-24
申请号：JP2012230565
申请日：2012-10-18
申请人： Merck Sharp & Dohme Corp , メルク・シャープ・アンド・ドーム・コーポレーションMerck Sharp & Dohme Corp. , Albany Molecular Research Inc , アルバニーモレキュラーリサーチ, インコーポレイテッド
发明人： TING PAULINE C , ASLANIAN ROBERT G , CAO JIANHUA , KIM DAVID WON-SHIK , KUANG RONGZE , ZHOU GANG , HERR ROBERT JASON , ZYCH ANDREW JOHN , YANG JINHAI , WU HEPING , ZORN NICOLAS
IPC分类号： C07D237/22 , A61K31/501 , A61K31/506 , A61K31/5377 , A61K31/675 , A61K31/695 , A61K31/7024 , A61K31/7034 , A61P31/10 , A61P31/12 , A61P43/00 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/04 , C07D405/12 , C07D407/04 , C07D407/12 , C07D407/14 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/04 , C07D417/12 , C07D417/14 , C07D471/10 , C07D487/04 , C07D487/08 , C07D515/08 , C07F9/6558 , C07H5/06 , C07H15/23 , C12N9/99
CPC分类号： C07D401/14 , C07D403/04 , C07D403/14 , C07D407/14 , C07D409/14 , C07D413/14 , C07D487/08 , C07D515/22
摘要： PROBLEM TO BE SOLVED: To provide pyridazinone derivatives useful as glucan synthase inhibitors.SOLUTION: In its many embodiments, the present invention provides: substituted pyridazinone compounds as glucan synthase inhibitors; methods of preparing such compounds; pharmaceutical including one or more of such compounds; methods of preparing pharmaceutical formulations including one or more such compounds or one or more such compounds along with other antifungal agents; and methods of treatment, prevention, inhibition, or amelioration of one or more fungal infections associated with glucan synthase using such compounds or pharmaceutical compositions.
摘要翻译：待解决的问题：提供可用作葡聚糖合酶抑制剂的哒嗪酮衍生物。解决方案：在其许多实施方案中，本发明提供：作为葡聚糖合酶抑制剂的取代的哒嗪酮化合物; 制备这些化合物的方法; 包括一种或多种这样的化合物的药物; 包括一种或多种这样的化合物或一种或多种这样的化合物以及其它抗真菌剂的药物制剂的方法; 以及使用这些化合物或药物组合物治疗，预防，抑制或改善与葡聚糖合酶相关的一种或多种真菌感染的方法。版权所有（C）2013，JPO＆INPIT

3. 发明申请

WO2015017393A2 PIPERAZINE DERIVATIVES AS HIV PROTEASE INHIBITORS 审中-公开
标题翻译：作为HIV蛋白酶抑制剂的哌嗪衍生物
公开(公告)号：WO2015017393A2
公开(公告)日：2015-02-05
申请号：PCT/US2014048581
申请日：2014-07-29
申请人： MERCK SHARP & DOHME , MSD R & D CHINA CO LTD , WILLIAMS PETER D , MCCAULEY JOHN A , BENNETT DAVID J , BUNGARD CHRISTOPHER J , CHANG LEHUA , CHU XIN-JIE , DWYER MICHAEL P , HOLLOWAY M KATHERINE , KEERTIKAR KARTIK M , LOUGHRAN H MARIE , MANIKOWSKI JESSE J , MORRIELLO GREGORI J , SHEN DONG-MING , SHERER EDWARD C , SCHULZ JUERGEN , WADDELL SHERMAN TIM , WISCOUNT CATHERINE M , ZORN NICOLAS , SATYANARAYANA TUMMANAPALLI , VIJAYASARADHI SIVALENKA , HU BIN , JI TAO , ZHONG BIN
发明人： WILLIAMS PETER D , MCCAULEY JOHN A , BENNETT DAVID J , BUNGARD CHRISTOPHER J , CHANG LEHUA , CHU XIN-JIE , DWYER MICHAEL P , HOLLOWAY M KATHERINE , KEERTIKAR KARTIK M , LOUGHRAN H MARIE , MANIKOWSKI JESSE J , MORRIELLO GREGORI J , SHEN DONG-MING , SHERER EDWARD C , SCHULZ JURGEN , WADDELL SHERMAN TIM , WISCOUNT CATHERINE M , ZORN NICOLAS , SATYANARAYANA TUMMANAPALLI , VIJAYASARADHI SIVALENKA , HU BIN , JI TAO , ZHONG BIN
IPC分类号： A61K31/496
CPC分类号： C07D241/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/14
摘要： The present invention is directed to piperazine derivatives, pharmaceutical compositions comprising the same, and their use in the inhibition of HIV protease, the inhibition of HIV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS.
摘要翻译：本发明涉及哌嗪衍生物，包含它们的药物组合物及其在抑制HIV蛋白酶，HIV复制抑制，HIV预防感染，HIV感染治疗和预防治疗中的用途，并延迟艾滋病的发病或进展。

4. 发明申请

WO2014123795A3 TETRACYCLIC HETEROCYCLE COMPOUNDS AND METHODS OF USE THEREOF FOR THE TREATMENT OF HEPATITIS C 审中-公开
标题翻译：四环杂环化合物及其用于治疗丙型肝炎的方法
公开(公告)号：WO2014123795A3
公开(公告)日：2014-10-30
申请号：PCT/US2014014365
申请日：2014-02-03
申请人： MERCK SHARP & DOHME , HE SHUWEN , DAI XING , PALANI ANANDAN , NARGUND RAVI , LAI ZHONG , ZORN NICOLAS , XIAO DONG , DANG QUN , LI PENG , PENG XUANJIA , SOLL RICHARD
发明人： HE SHUWEN , DAI XING , PALANI ANANDAN , NARGUND RAVI , LAI ZHONG , ZORN NICOLAS , XIAO DONG , DANG QUN , LI PENG , PENG XUANJIA , SOLL RICHARD
IPC分类号： A01N43/42 , A61K31/44
CPC分类号： C07D498/14 , A61K31/5365 , A61K31/5377 , A61K45/06 , A61K2300/00
摘要： The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system. I
摘要翻译：本发明涉及可用作丙型肝炎病毒（HCV）NS5B聚合酶抑制剂，此类化合物的合成，以及此类化合物用于抑制HCV NS5B聚合酶活性的用途的式（I）化合物，用于治疗或预防HCV感染并用于在基于细胞的系统中抑制HCV病毒复制和/或病毒产生。一世

5. 发明申请

WO2013130370A2 COMPOUNDS AS DGAT-1 INHIBITORS 审中-公开
标题翻译：化合物作为DGAT-1抑制剂
公开(公告)号：WO2013130370A2
公开(公告)日：2013-09-06
申请号：PCT/US2013027548
申请日：2013-02-25
申请人： MERCK SHARP & DOHME , DEVITA ROBERT J , YU YANG , LIU JIAN , HE SHUWEN , KRIKORIAN ARTO D , MILLER DANIEL J , WU ZHICAI , YANG GINGER XU-QIANG , HONG QUINGMEI , LAI ZHONG , ZORN NICOLAS , TING PAULINE C
发明人： DEVITA ROBERT J , YU YANG , LIU JIAN , HE SHUWEN , KRIKORIAN ARTO D , MILLER DANIEL J , WU ZHICAI , YANG GINGER XU-QIANG , HONG QUINGMEI , LAI ZHONG , ZORN NICOLAS , TING PAULINE C
IPC分类号： A61K31/513
CPC分类号： C07D401/14 , C07D235/18 , C07D401/10 , C07D403/10 , C07D403/14 , C07D417/14 , C07D471/04
摘要： Described herein are compounds of formula I. The compounds of formula I act as DGAT1 inhibitors and can be useful in preventing, treating or acting as a remedial agent for hyperlipidemia, diabetes mellitus and obesity.
摘要翻译：本文描述了式I化合物。式I化合物起DGAT1抑制剂的作用，可用于预防，治疗或作为高脂血症，糖尿病和肥胖症的治疗剂。

6. 发明专利

CA2896056C HETEROBICYCLO-SUBSTITUTED-[1,2,4]TRIAZOLO[1,5-C]QUINAZOLIN-5-AMINE COMPOUNDS WITH A2A ANTAGONIST PROPERTIES 未知
公开(公告)号：CA2896056C
公开(公告)日：2020-11-10
申请号：CA2896056
申请日：2013-12-20
申请人： MERCK SHARP & DOHME
发明人： ALI AMJAD , LO MICHAEL MAN-CHU , LIM YEON-HEE , STAMFORD ANDREW , KUANG RONGZE , TEMPEST PAUL , YU YOUNONG , HUANG XIANHAI , HENDERSON TIMOTHY J , KIM JAE-HUN , BOYCE CHRISTOPHER , TING PAULINE , ZHENG JUNYING , METZGER EDWARD , ZORN NICOLAS , XIAO DONG , GALLO GIOCONDA V , WON WALTER , WU HEPING , DENG QIAOLIN
IPC分类号： C07D519/00 , A61K31/517 , A61K31/519 , A61K31/55 , A61P25/00 , A61P25/16 , C07D487/04
摘要： Disclosed are compounds of Formula Gl (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.

7. 发明专利

CY1120258T1 ΕΝΩΣΕΙΣ ΕΤΕΡΟΔΙΚΥΚΛΟ-ΥΠΟΚΑΤΕΣΤΗΜΕΝΗΣ-[1,2,4]ΤΡΙΑΖΟΛΟ [1,5-C]ΚΙΝΑΖΟΛΙΝ-5-ΑΜΙΝΗΣ ΚΑΤΑΛΛΗΛΕΣ ΓΙΑ ΑΓΩΓΗ Ή ΠΡΟΛΗΨΗ ΔΙΑΤΑΡΑΧΩΝ ΤΟΥ ΚΕΝΤΡΙΚΟΥ ΝΕΥΡΙΚΟΥ ΣΥΣΤΗΜΑΤΟΣ 未知
公开(公告)号：CY1120258T1
公开(公告)日：2019-07-10
申请号：CY181100472
申请日：2018-05-04
申请人： MERCK SHARP & DOHME
发明人： ALI AMJAD , LO MICHAEL MAN-CHU , LIM YEON-HEE , STAMFORD ANDREW , KUANG RONGZE , TEMPEST PAUL , YU YOUNONG , HUANG XIANHAI , HENDERSON TIMOTHY J , KIM JAE-HUN , BOYCE CHRISTOPHER , TING PAULINE , ZHENG JUNYING , METZGER EDWARD , ZORN NICOLAS , XIAO DONG , GALLO GIOCONDA V , WON WALTER , WU HEPING , DENG QIAOLIN
IPC分类号： C07D487/04 , A61K31/4985 , A61K31/519 , A61P25/16
摘要： ΑποκαλύπτονταιενώσειςτουΧημικούΤύπου GI (πουαναπαρίστανταιδομικώς): όπουτα "RG3" "Rd1" έως "Rd4", "n", "m", "p", "W", "Χ", και "Ζ" καθορίζονταιειςτοπαρόνοιοποίεςενώσειςείναιανταγωνιστέςτουυποδοχέαΑ2Α. Αποκαλύπτονταιεπίσηςειςτοπαρόνκαιχρήσειςτωνενώσεωνπουπεριγράφονταιειςτοπαρόνωςανταγωνιστέςτουυποδοχέα A2a στηδυνητικήαγωγήή πρόληψηνευρολογικώνδιαταραχώνκαιπαθήσεωνστιςοποίεςοιυποδοχείςΑ2Αενέχονται. Αποκαλύπτονταιεπίσηςειςτοπαρόνκαιφαρμακευτικέςσυνθέσειςπουπεριλαμβάνουναυτέςτιςενώσειςκαιχρήσειςαυτώντωνφαρμακευτικώνσυνθέσεων.

9. 发明专利

ES2667477T3 Compuestos heterobiciclo-sustituidos-[1,2,4]triazolo[1,5-c]quinazolin-5-amina adecuados para el tratamiento o la prevención de trastornos del sistema nervioso central 未知
公开(公告)号：ES2667477T3
公开(公告)日：2018-05-11
申请号：ES13866588
申请日：2013-12-20
申请人： MERCK SHARP & DOHME
发明人： ALI AMJAD , LO MICHAEL MAN-CHU , LIM YEON-HEE , STAMFORD ANDREW , KUANG RONGZE , TEMPEST PAUL , YU YOUNONG , HUANG XIANHAI , HENDERSON TIMOTHY , KIM JAE-HUN , BOYCE CHRISTOPHER , TING PAULINE , ZHENG JUNYING , METZGER EDWARD , ZORN NICOLAS , XIAO DONG , GALLO GIOCONDA , WON WALTER , WU HEPING , DENG QIAOLIN
IPC分类号： C07D487/04 , A61K31/4985 , A61K31/519 , A61P25/16
摘要： compuesto de Fórmula GI:***Fórmula** o una de sus sales farmacéuticamente aceptables, en la que: W es nitrógeno o carbono; m es 1, 2, 3 o 4; n es un número entero de 0 a 4, en donde la suma de n + m es al menos 2 hasta 4, y en donde, cuando W es N, m es al menos 2; Gd1 a Gd4 son independientemente hidrógeno o un alquilo C1-6; p es 1 o 2; X, Y y Z junto con W y el carbono al que están enlazados X y W forman un resto aromático o heteroaromático de 5 a 6 miembros, y son independientemente: (a) -(RG1)C>=, en el que RG1 es: (i) hidrógeno; (ii) alquilo C1-8, opcionalmente sustituido con uno o más átomos de halógeno; (iii) -C(O)-alquilo C1-8; (iv) -CN; (v) -S-alquilo C1-8; (vi) -O-alquilo C1-6; (vii) -(CH2)q1-(C>=O)q2-N(R2)2, donde R2 25 es independientemente cada vez que aparece hidrógeno, alquilo C1-6 o heteroarilo, y en donde q1 es 0 o 1 y q2 es 0 o 1; (viii) -C(O)O-alquilo C1-8; (ix) halógeno; (x) un resto heterocíclico mono o policíclico que comprende hasta 10 átomos de carbono y uno o más heteroátomos seleccionados entre N, S u O, opcionalmente sustituido con uno o más alquilo C1-6, morfolino, fenilo (opcionalmente sustituido con halógeno), heteroarilo o halógeno; (xi) arilo, que está opcionalmente sustituido con uno o más sustituyentes que son: (1) halógeno; o (2) alquilo C1-6 que está opcionalmente sustituido con uno o más átomos de halógeno; (xii) -NH-C(O)-R3, en el que R3 es alquilo C1-6 o heteroarilo; o (xiii) heteroarilo, que está opcionalmente sustituido con alquilo C1-6 (que está opcionalmente sustituido con uno o más átomos de halógeno) o amino; o (b) >NRG2, en el que RG2 es: (i) hidrógeno; (ii) alquilo C1-8; o (iii) un resto aromático de hasta 10 átomos de carbono; (c) -N>=; (d) -O-; o (e) -S-; y RG3 es un resto de la estructura:**Fórmula** en la que: t es 0, 1 o 2; RG5 y RG6 son independientemente cada vez que aparecen: (a) H; (b) alquilo C1-10, opcionalmente sustituido con uno o más átomos de flúor; o (c) RG5 y RG6 tomados juntos forman un resto carbonilo (C>=O), con la condición de que si t >= 2, RG5 y RG6 no se seleccionan para proporcionar dos restos carbonilo adyacentes; y RGa1 es de 1 a 3 sustituyentes que reemplazan un H en un átomo de carbono del anillo, que son independientemente cada vez que aparecen: (a) alcoxi C1-4, en donde la porción de alquilo del resto alcoxi está opcionalmente sustituida con uno o más halógenos; (b) alquilo C1-8, opcionalmente sustituido con uno o más átomos de halógeno; (c) halógeno; (d) -CN; o (e) -N(RG4)2, en el que al menos uno de RG4 es alquilo C1-6 y el otro es H o alquilo C1-6.

10. 发明专利

AU2008227100B2 Pyridazinone derivatives useful as glucan synthase inhibitors 未知
公开(公告)号：AU2008227100B2
公开(公告)日：2014-01-09
申请号：AU2008227100
申请日：2008-03-12
申请人： ALBANY MOLECULAR RES INC , MERCK SHARP & DOHME
发明人： ASLANIAN ROBERT G , ZYCH ANDREW JOHN , YANG JINHAI , CAO JIANHUA , HERR ROBERT JASON , ZORN NICOLAS , ZHOU GANG , TING PAULINE C , WU HEPING , KIM DAVID WON-SHIK , KUANG RONGZE
IPC分类号： C07D401/14 , A61K31/501 , A61P31/00 , C07D403/04 , C07D403/14 , C07D407/14 , C07D409/14 , C07D413/14 , C07D487/08 , C07D515/22
摘要： In its many embodiments, the present invention provides -substituted pyridazinone compounds as glucan synthase inhibitors, methods of preparing such compounds, pharmaceutical including one or more of such compounds, methods of preparing pharmaceutical formulations including one or more such compounds or one or more such compounds along with other antifungal agents, and methods of treatment, prevention, inhibition, or amelioration of one or more fungal infections associated with glucan synthase using such compounds or pharmaceutical compositions.

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