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61. 发明申请

WO2016105468A1 DERIVATIVES OF 3-HETEROARYLISOXAZOL-5-CARBOXYLIC AMIDE USEFUL FOR THE TREATMENT OF INTER ALIA CYSTIC FIBROSIS 审中-公开
标题翻译： 3-异羟肟酸-5-羧酰胺的衍生物有助于治疗间质性纤维蛋白样变
公开(公告)号：WO2016105468A1
公开(公告)日：2016-06-30
申请号：PCT/US2015/000189
申请日：2015-12-23
申请人： PROTEOSTASIS THERAPEUTICS, INC.
发明人： BASTOS, Cecilia, M. , MUNOZ, Benito , TAIT, Bradley
IPC分类号： C07D413/12 , C07D417/12 , A61K31/4155 , A61K31/4192 , A61K31/42 , A61K31/4245 , A61K31/433 , A61P11/00 , A61P37/00
CPC分类号： C07D413/14 , C07D413/12 , C07D417/12
摘要： The present disclosure is based, in part, on the discovery that disclosed compounds can increase cystic fibrosis transmembrane conductance regulator (CFTR) activity as measured in human bronchial epithelial (hBE) cells.
摘要翻译：本公开部分地基于所公开的化合物可以增加在人支气管上皮（hBE）细胞中测量的囊性纤维化跨膜传导调节物（CFTR）活性的发现。

62. 发明申请

WO2016102435A2 NOVEL ISOTHIAZOLAMIDES, PROCESSES FOR THEIR PREPARATION AND THEIR USE AS FUNGICIDES 审中-公开
标题翻译：新型异噻菌胺，其制备方法及其作为杀真菌剂的用途
公开(公告)号：WO2016102435A2
公开(公告)日：2016-06-30
申请号：PCT/EP2015080739
申请日：2015-12-21
申请人： BAYER CROPSCIENCE AG
发明人： BERNIER DAVID , CRISTAU PIERRE , TSUCHIYA TOMOKI , RINOLFI PHILIPPE , DRÖGE THOMAS , MAECHLING SIMON , SCHMIDT JAN PETER , TELSER JOACHIM , DÖLLER UWE , MOSRIN MARC , REY JULLIEN , TIEBES JÖRG , WACHENDORFF-NEUMANN ULRIKE
IPC分类号： A01N43/80 , A01P3/00 , C07D275/03
CPC分类号： A01N43/80 , A01N47/18 , C07D275/03 , C07D417/12
摘要： The present invention relates to novel isothiazolamide derivatives, to processes for preparing these compounds, to compositions comprising these compounds, and to the use thereof as biologically active compounds for controlling harmful microorganisms in crop protection and in the protection of materials, especially for controlling fungi, preferably for controlling fungi in plants or plant seeds.
摘要翻译：本发明涉及新型异噻唑酰胺衍生物，涉及制备这些化合物的方法，涉及包含这些化合物的组合物，并且涉及其作为生物活性化合物用于防治作物保护中的有害微生物和保护材料，尤其是防治真菌的用途，优选用于控制植物或植物种子中的真菌。

63. 发明申请

WO2016097071A1 ESTROGEN RECEPTOR MODULATORS AND USES THEREOF 审中-公开
标题翻译：雌激素受体调节剂及其用途
公开(公告)号：WO2016097071A1
公开(公告)日：2016-06-23
申请号：PCT/EP2015/080118
申请日：2015-12-17
申请人： F. HOFFMANN-LA ROCHE AG , GENENTECH, INC.
发明人： SMITH, Nicholas D. , LIANG, Jun , ORTWINE, Daniel Fred , WANG, Xiaojing , KAHRAMAN, Mehmet , NAGASAWA, Johnny Y. , GOODACRE, Simon Charles , RAY, Nicholas Charles , GOVEK, Steven P.
IPC分类号： C07D401/14 , A61K31/397 , A61K31/4025 , C07D403/02 , C07D403/14 , C07D409/02 , C07D413/02 , C07D417/02 , C07D417/14 , C07D205/04 , C07D207/08 , C07D493/04 , C07D411/02
CPC分类号： C07D205/04 , A61K31/381 , A61K31/397 , A61K31/40 , A61K31/4025 , A61K31/404 , A61K31/416 , A61K31/422 , A61K31/426 , A61K31/427 , A61K31/4439 , A61K31/5415 , A61K45/06 , C07D207/04 , C07D207/08 , C07D401/14 , C07D403/02 , C07D403/12 , C07D403/14 , C07D409/02 , C07D409/12 , C07D411/02 , C07D411/12 , C07D413/02 , C07D413/12 , C07D417/02 , C07D417/12 , C07D417/14 , C07D493/04 , A61K2300/00
摘要： Described herein are compounds that are estrogen receptor modulators of Formula (I) and stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein SERMF is a selective estrogen receptor modulator fragment and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.
摘要翻译：本文描述的是式（I）的雌激素受体调节剂和其立体异构体，互变异构体或其药学上可接受的盐的化合物，其中SERMF是选择性雌激素受体调节剂片段，并且具有本文所述的取代基和结构特征。还描述了包括本文所述化合物的药物组合物和药物，以及使用这种雌激素受体调节剂单独使用并与其它化合物联合用于治疗介导或依赖于雌激素受体的疾病或病症的方法。

64. 发明申请

WO2016096126A1 1-METHYLPYRAZOLE-PIPERAZINE COMPOUNDS HAVING MULTIMODAL ACTIVITY AGAINST PAIN 审中-公开
标题翻译：具有多种药物活性的1-甲基吡唑 - 哌嗪化合物
公开(公告)号：WO2016096126A1
公开(公告)日：2016-06-23
申请号：PCT/EP2015/002525
申请日：2015-12-15
申请人： LABORATORIOS DEL DR. ESTEVE, S.A.
发明人： ALMANSA-ROSALES, Carmen , GARCIA-LOPEZ, Monica , GARRIGA-SANAHUJA, Lourdes
IPC分类号： C07D401/14 , A61K31/4523 , A61K31/496 , C07D403/06 , C07D417/14
CPC分类号： C07D417/12 , A61K31/4523 , A61K31/496 , C07D231/12 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D417/14
摘要： The present invention relates to 1-methylpyrazole-piperazine compounds having dual pharmacological activity towards both the sigma (σ) receptor, and the μ-opiod receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain.
摘要翻译：本发明涉及对西格玛（σ）受体和μ-阿片受体两者具有双重药理活性，制备这些化合物的方法，包括它们的药物组合物的1-甲基吡唑 - 哌嗪化合物及其在治疗，特别是治疗疼痛。

65. 发明申请

WO2016094688A1 FUSED 1,3-AZOLE DERIVATIVES USEFUL FOR THE TREATMENT OF PROLIFERATIVE DISEASES 审中-公开
标题翻译：用于治疗增殖性疾病的1,3佐剂衍生物
公开(公告)号：WO2016094688A1
公开(公告)日：2016-06-16
申请号：PCT/US2015/065044
申请日：2015-12-10
申请人： MASSACHUSETTS INSTITUTE OF TECHNOLOGY
发明人： KOEHLER, Angela, N. , STEFAN, Eric , CABALLERO, Francisco
IPC分类号： C07D405/14 , C07D405/12 , C07D417/12 , C07D417/14 , C07D495/04 , A61K31/404 , A61K31/407 , A61K31/4184 , A61K31/4188 , A61P35/02
CPC分类号： C07D495/04 , C07D405/12 , C07D405/14 , C07D417/12 , C07D417/14 , C07D471/04
摘要： The present disclosure provides compounds of Formula (I-a), Formula (I), and Formula (II),. The compounds described herein may be Myc modulators ( e.g ., Myc inhibitors) and may be useful in treating in a subject in need thereof diseases associated with Myc and proliferative diseases ( e.g ., cancer). Also provided in the present disclosure are pharmaceutical compositions, kits, methods, and uses including a compound described herein. (Formulae (I-a), (I), (II))
摘要翻译：本公开提供式（I-a），式（I）和式（II）的化合物。本文所述的化合物可以是Myc调节剂（例如，Myc抑制剂），并且可用于治疗有需要的受试者与Myc和增殖性疾病（例如癌症）相关的疾病。在本公开中还提供了药物组合物，试剂盒，方法和用途，包括本文所述的化合物。（式（I-a），（I），（II））

66. 发明申请

WO2016087265A1 PESTICIDALLY ACTIVE AMIDE HETEROCYCLIC DERIVATIVES WITH SULPHUR CONTAINING SUBSTITUENTS 审中-公开
标题翻译：具有硫含量替代物的农药活性酰胺杂环衍生物
公开(公告)号：WO2016087265A1
公开(公告)日：2016-06-09
申请号：PCT/EP2015/077469
申请日：2015-11-24
申请人： SYNGENTA PARTICIPATIONS AG
发明人： MUEHLEBACH, Michel , EDMUNDS, Andrew , JEANGUENAT, André , JUNG, Pierre Joseph Marcel , RENOLD, Peter , HUETER, Ottmar Franz
IPC分类号： C07D417/12 , A01N43/824
CPC分类号： C07D417/14 , A01N43/82 , C07D417/12
摘要： Compounds of formula (I), wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts, stereoisomers, enantiomers, tautomers and N-oxides of those compounds, can be used as insecticides and can be prepared in a manner known per se.
摘要翻译：其中取代基如权利要求1中定义的式（I）化合物和这些化合物的农业化学上可接受的盐，立体异构体，对映异构体，互变异构体和N-氧化物可用作杀虫剂，并且可以以已知的方式制备 SE。

67. 发明申请

WO2015179559A3 PYRAZOLE COMPOUNDS AND METHODS OF MAKING AND USING SAME 审中-公开
标题翻译：吡咯化合物及其制备方法和使用方法
公开(公告)号：WO2015179559A3
公开(公告)日：2016-06-09
申请号：PCT/US2015031834
申请日：2015-05-20
申请人： ABIDE THERAPEUTICS INC , SCRIPPS RESEARCH INST
发明人： BOGER DALE L , OTRUBOVA KATERINA , CISAR JUSTIN S , GRICE CHERYL A , JONES TODD K
IPC分类号： C07D403/06 , A61K31/4155 , A61P25/28 , A61P29/00 , A61P35/00 , C07D231/10 , C07D403/14 , C07D413/14
CPC分类号： C07D231/14 , C07D231/12 , C07D231/16 , C07D401/12 , C07D403/12 , C07D405/12 , C07D417/12 , C07D491/10 , C07D491/107
摘要： Provided herein are pyrazole compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful as modulators of one or more of MAGL, ABHD6, and FAAH. Furthermore, the subject compounds and compositions are useful for the treatment of, for example, pain, solid tumors and/or obesity.
摘要翻译：本文提供的是吡唑化合物和包含所述化合物的药物组合物。主题化合物和组合物可用作MAGL，ABHD6和FAAH中的一种或多种的调节剂。此外，本发明化合物和组合物可用于治疗例如疼痛，实体瘤和/或肥胖症。

68. 发明申请

WO2016081464A1 MONOCARBOXYLATE TRANSPORT MODULATORS AND USES THEREOF 审中-公开
标题翻译：单羧酸交联调节剂及其用途
公开(公告)号：WO2016081464A1
公开(公告)日：2016-05-26
申请号：PCT/US2015/061101
申请日：2015-11-17
申请人： NIROGYONE THERAPEUTICS, INC.
发明人： SANDANAYAKA, Vincent , WU, Qiong
IPC分类号： C07D215/56 , A61K31/435 , C07D401/06
CPC分类号： A61K31/435 , C07D215/56 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D471/04
摘要： The invention generally relates to the field of monocarboxylate transport modulators, e.g., monocarboxylate transport inhibitors, and more particularly to new substituted-quinolone compounds, the synthesis and use of these compounds and their pharmaceutical compositions, e.g., in treating, modulating, forestalling and/or reducing physiological conditions associated with monocarboxylate transport activity such as in treating cancer and other neoplastic disorders, inflammatory diseases, disorders of abnormal tissue growth and fibrosis including cardiomyopathy, obesity, diabetes, cardiovascular diseases, tissue and organ transplant rejection, and malaria.
摘要翻译：本发明一般涉及单羧酸盐转运调节剂领域，例如单羧酸盐转运抑制剂，更具体地涉及新的取代的喹诺酮化合物，这些化合物及其药物组合物的合成和用途，例如在治疗，调节，预防和/ 或减少与单羧酸转运活性相关的生理条件，例如治疗癌症和其它肿瘤性疾病，炎症性疾病，异常组织生长障碍和包括心肌病，肥胖症，糖尿病，心血管疾病，组织和器官移植排斥反应以及疟疾在内的纤维化。

69. 发明申请

WO2016071293A2 PHARMACEUTICAL COMPOUND 审中-公开
标题翻译：药用化合物
公开(公告)号：WO2016071293A2
公开(公告)日：2016-05-12
申请号：PCT/EP2015075486
申请日：2015-11-02
申请人： IOMET PHARMA LTD
发明人： COWLEY PHILLIP , WISE ALAN
IPC分类号： A61K31/4985
CPC分类号： A61K31/4985 , A61K31/416 , A61K31/438 , A61K31/439 , A61K31/445 , A61K31/4523 , A61K31/454 , A61K31/496 , A61K31/499 , A61K31/4995 , C07D231/56 , C07D261/20 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/06 , C07D417/12 , C07D417/14 , C07D471/04 , C07D471/08 , C07D471/10 , C07D487/04 , C07D498/04 , C07D498/08 , C07D498/10
摘要： Provided is a tryptophan-2,3-dioxygenase (TDO) and/or indoleamine-2,3-dioxygenase (IDO) inhibitor compound for use in medicine, which compound comprises formula (I) wherein X1, and X2 may be the same or different and each is independently selected from C, N, O and S; X3, X4, X5, and X6 may be the same or different and each is independently selected from C and N; each bond represented by a dotted line may be present or absent, provided that at least one such bond is present; R1, R2, R3, R4, R5 and R6 may be present or absent and may be the same or different and each is independently selected from H and a substituted or unsubstituted organic group, provided that the number of R1, R2, R3, R4, R5 and R6 groups present is such that the respective valencies of X1, X2, X3, X4, X5, and X6 are maintained; and wherein at least one of R5 and R6 comprises a group Y, wherein Y is a group having a formula selected from (II), (III), (IV), (V), (VI), (VII) wherein L may be present or absent, and may be a substituted or unsubstituted organic linking group; R31 and R32 may be the same or different and are selected from H and a substituted or unsubstituted organic group; each R34 may be the same or different and is selected from H and a substituted or unsubstituted organic group; R35 is selected from a substituted or unsubstituted alcohol group or ether group; each R36 may be the same or different and is selected from H and a substituted or unsubstituted organic group; X7 may be selected from C and N; X8, X9, X10, X11, X12, X13, X14, X15 and X16 may be the same or different and each is independently selected from C, N, O and S; each bond represented by a dotted line may be present or absent; and each R313 may be the same or different and is selected from H and a substituted or unsubstituted organic group.
摘要翻译：提供了用于药物的色氨酸-2,3-双加氧酶（TDO）和/或吲哚胺-2,3-双加氧酶（IDO）抑制剂化合物，该化合物包含式（I），其中X 1和X 2可以相同或各自独立地选自C，N，O和S; X3，X4，X5和X6可以相同或不同，并且各自独立地选自C和N; 由虚线表示的每个键可以存在或不存在，条件是存在至少一个这样的键; R 1，R 2，R 3，R 4，R 5和R 6可以存在或不存在，并且可以相同或不同，并且各自独立地选自H和取代或未取代的有机基团，条件是R 1，R 2，R 3，R 4 存在的R 5和R 6基团使得保持X 1，X 2，X 3，X 4，X 5和X 6的各自的价数; 并且其中R 5和R 6中的至少一个包含基团Y，其中Y是具有选自（II），（III），（IV），（V），（VI），（VII）的式的基团，其中L可以存在或不存在，并且可以是取代或未取代的有机连接基团; R 31和R 32可以相同或不同，并且选自H和取代或未取代的有机基团; 每个R 34可以相同或不同，并且选自H和取代或未取代的有机基团; R35选自取代或未取代的醇基或醚基; 每个R 36可以相同或不同，并且选自H和取代或未取代的有机基团; X7可以选自C和N; X 8，X 9，X 10，X 11，X 12，X 13，X 14，X 15和X 16可以相同或不同，并且各自独立地选自C，N，O和S; 由虚线表示的每个键可以存在或不存在; 并且每个R 13可以相同或不同，并且选自H和取代或未取代的有机基团。

70. 发明申请

WO2016066696A1 DERIVATIVES OF 2-(1,2,4-TRIAZOL-3-YLSULFANYL)-N-1,3,4-THIADIAZOL-2-YL ACETAMIDE WHICH ARE USEFUL FOR THE TREATMENT OF INTER ALIA DIABETES 审中-公开
标题翻译：可用于治疗糖尿病的2-（1,2,4-三唑-3-基磺酰基）-N-1,3,4-噻二唑-2-基乙酰胺的衍生物
公开(公告)号：WO2016066696A1
公开(公告)日：2016-05-06
申请号：PCT/EP2015/075007
申请日：2015-10-28
申请人： APOGLYX AB
发明人： RÜTZLER, Michael , BRIMERT, Thomas , DREISCH, Klaus , EVENÄS, Johan , LARSSON, Joakim
IPC分类号： C07D417/12 , C07D417/14 , A61K31/4439 , A61K31/433 , A61P3/10 , A61P13/12 , A61P37/00
CPC分类号： C07D417/12 , A61K31/4196 , A61K31/433 , C07D249/12 , C07D285/135 , C07D403/12 , C07D417/14
摘要： Disclosed are compounds, pharmaceutical compositions and methods for modulating aquaporin 9.
摘要翻译：公开了用于调节水通道蛋白的化合物，药物组合物和方法9。

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