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1. 发明申请

WO2015112014A1 PROCESS FOR THE CYCLOADDITION OF A HETERO(ARYL) 1,3-DIPOLE COMPOUND WITH A (HETERO)CYCLOALKYNE 审中-公开
标题翻译：环己酮（ARYL）1,3-二烯化合物与（环己基）环烷酮的环化方法
公开(公告)号：WO2015112014A1
公开(公告)日：2015-07-30
申请号：PCT/NL2015/050045
申请日：2015-01-26
申请人： STICHTING KATHOLIEKE UNIVERSITEIT
发明人： VAN DELFT, Floris Louis , DOMMERHOLT, Frederik Jan
IPC分类号： C07D225/02 , C07D225/08 , C07D231/54 , C07D249/16 , C07D261/20 , C07H19/10 , A61K47/48
CPC分类号： C07D487/04 , A61K47/48061 , A61K47/48215 , A61K47/48584 , A61K47/545 , A61K47/60 , A61K47/6855 , C07C269/06 , C07C271/18 , C07C2602/22 , C07C2603/50 , C07D225/02 , C07D225/08 , C07D231/54 , C07D249/16 , C07D261/20 , C07H19/10 , C07K14/473
摘要： The present invention relates to a process comprising the step of reacting a (hetero)aryl 1,3-dipole compound with a (hetero)cycloalkyne, wherein: a (hetero)aryl 1,3-dipole compound is defined as a compound comprising a 1,3-dipole functional group, wherein the 1,3-dipole functional group is bonded to a (hetero)aryl group, and wherein the (hetero)aryl 1,3-dipole compound is a (hetero)aryl azide or a (hetero)aryl diazo compound; wherein: (i) the (hetero)aryl group of the (hetero)aryl 1,3-dipole compound comprises one or more substituents having a positive value for the para -Hammett substituent constant σ p and/or the meta -Hammett substituent constant σ m , and/or (ii) the (hetero)aryl group of the (hetero)aryl 1,3-dipole compound is an electron-poor (hetero)aryl group, wherein an electron-poor (hetero)aryl group is: (ii-a) a (hetero)aryl group wherein the (hetero)aromatic ring system is bearing a positive charge, and/or (ii-b) a (hetero)aryl group wherein the ratio {number of π-electrons present in the (hetero)aromatic ring system} : {number of protons present in the nuclei of the (hetero)aromatic ring system} is lower than 0.167 for a 6-membered ring, or lower than 0.200 for a 5-membered ring; and wherein the (hetero)cycloalkyne is a (hetero)cyclooctyne or a (hetero)cyclononyne according to Formula (1): The invention also relates to the products obtainable by the process according to the invention.
摘要翻译：本发明涉及包括使（杂）芳基-1,3-偶极化合物与（异）环炔反应的步骤的方法，其中：（杂）芳基-1,3-偶极化合物定义为包含 1,3-偶极官能团，其中1,3-偶极官能团与（杂）芳基键合，其中（杂）芳基1,3-偶极化合物是（杂）芳基叠氮化物或（杂）杂）芳基重氮化合物; 其中：（i）（杂）芳基1,3-偶极化合物的（杂）芳基包含一个或多个对位 - 哈米特取代基常数σp和/或间 - 哈米特取代基常数σm具有正值的取代基，（ii）（杂）芳基-1,3-偶极子化合物的（杂）芳基是电子贫（杂）芳基，其中电子贫（杂）芳基是：（ii -a）（杂）芳环体系带有正电荷的（杂）芳基，和/或（ii-b）（杂）芳基，其中存在于（杂）芳环体系}：（杂）芳环体系的核中存在的质子数目对于6元环低于0.167，对于5元环低于0.200; 并且其中（杂）环炔是根据式（1）的（杂）环辛炔或（杂）环壬烯：本发明还涉及通过本发明的方法获得的产物。

2. 发明申请

WO2010050781A1 NOVEL ORGANIC ELECTROLUMINESCENT COMPOUNDS AND ORGANIC ELECTROLUMINESCENT DEVICE USING THE SAME 审中-公开
标题翻译：新型有机电致发光化合物和使用该有机电致发光化合物的有机电致发光器件
公开(公告)号：WO2010050781A1
公开(公告)日：2010-05-06
申请号：PCT/KR2009/006353
申请日：2009-10-30
申请人： GRACEL DISPLAY INC. , CHO, Young Jun , KIM, Chi Sik , EUM, Sung Jin , KWON, Hyuck Joo , KIM, Bong Ok , KIM, Sung Min , YOON, Seung Soo
发明人： CHO, Young Jun , KIM, Chi Sik , EUM, Sung Jin , KWON, Hyuck Joo , KIM, Bong Ok , KIM, Sung Min , YOON, Seung Soo
IPC分类号： C07D401/10 , C07D401/14 , C07D221/06 , C07D225/08 , C07D241/46 , H01L51/00 , C07D221/02 , C07D265/38 , C07D279/18
CPC分类号： C09K11/06 , C07D215/06 , C07D279/22 , C07D401/04 , C07D401/10 , C07D401/14 , C07D417/10 , C07D417/14 , C09K2211/1011 , C09K2211/1014 , C09K2211/1022 , C09K2211/104 , H01L51/0058 , H01L51/006 , H01L51/5012 , H05B33/14 , Y02E10/549
摘要： Disclosed Provided are a novel organic electroluminescent compound and an organic electroluminescent device using the same as an electroluminescent material. The disclosed organic electroluminescent compound is represented by Chemical Formula 1: (Formula I should be inserted here) wherein Ar 1 represents (C6-C60)arylene, (C3~C60)heteroarylene containing one or more heteroatom(s) selected from N, O and S, 5- or 6-membered heterocycloalkylene containing one or more heteroatom(s) selected from N, O and S, (C3-C60)cycloalkylene, adamantylene, (C7-C60)bicycloalkylene, (C2-C60)alkenylene, (C2-C60)alkynylene, (Cl-C60)alkylenethio, (Cl-C60)alkyleneoxy, (C6-C60)aryleneoxy, (C6-C60)arylenethio or; (Formula II should be inserted here) and ring A and ring B independently represent a 5- to 7-membered heterocyclic amino group or a ring selected from the following structures: (Formula III should be inserted here) wherein the 5- to 7-membered heterocyclic amino group may further contain NR 2I or one or more heteroatom(s) selected from O and S. The organic electroluminescent compound provides superior luminous efficiency and excellent life property. Therefore, it may be used to manufacture OLED devices having very good operation life.
摘要翻译：公开了一种新的有机电致发光化合物和使用该有机电致发光化合物作为电致发光材料的有机电致发光器件。所公开的有机电致发光化合物由化学式1表示：（式I应在此插入），其中Ar 1表示（C 6 -C 60）亚芳基，（C 3 -C 60）亚杂芳基，其含有一个或多个选自N，O的杂原子和含有一个或多个选自N，O和S的杂原子，（C 3 -C 60）亚环烷基，金刚烷基，（C 7 -C 60）双亚烷基，（C 2 -C 60）亚烯基，（C 2 -C 60） -C 60）亚炔基，（C 1 -C 60）亚烷基硫代，（C 1 -C 60）亚烷基氧基，（C 6 -C 60）亚芳基氧基，（C 6 -C 60）（这里应该插入式II），环A和环B独立地表示5-至7-元杂环氨基或选自以下结构的环：（式III中应插入），其中5-至7-元杂环氨基或选自以下结构的环：可以进一步含有NR 2 I或选自O和S的一个或多个杂原子。有机电致发光化合物提供优异的发光效率和优异的寿命性质。因此，其可用于制造具有非常好的使用寿命的OLED器件。

3. 发明申请

WO2008145525A2 PROCESS FOR THE PREPARATION OF DIBENZO [B,D]AZEPIN-6-ONE DERIVATIVE 审中-公开
标题翻译：二苯并[B，D]亚氨基-6-酮衍生物的制备方法
公开(公告)号：WO2008145525A2
公开(公告)日：2008-12-04
申请号：PCT/EP2008/055937
申请日：2008-05-15
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-EMERY, Fabienne , JAKOB-ROETNE, Roland
发明人： HOFFMANN-EMERY, Fabienne , JAKOB-ROETNE, Roland
IPC分类号： C07D225/08
CPC分类号： C07D225/08
摘要： The invention relates to a process for the optical resolution of a dibenzo[b,d]azepinone derivative of the formula (II) wherein R 1 is hydrogen or halogen and R 2 has the meaning of C 1- 4 -alkyl optionally substituted with C 3-7 -cycloalkyl or benzyl which is optionally substituted with C 1-4 -alkoxy to obtain a (S)-7-amino-5H,7H-dibenzo[b,d]azepin-6-one of the formula (I) wherein R 1 is as above. The (S)-7-amino-5H,7H-dibenzo[b,d]azepin-6-ones of formula (I) can be used as chiral building blocks for the preparation of malonamide derivatives which have the potential to act as γ-secretase inhibitors and therefore may be useful in the treatment of Alzheimer's disease and cancer.
摘要翻译：本发明涉及一种用于光学拆分式（II）的二苯并[b，d]氮杂酮衍生物的方法，其中R 1是氢或卤素，并且R 2具有C1-

4. 发明申请

WO2007047737A1 CB-1 MODULATING COMPOUNDS AND THEIR USE 审中-公开
标题翻译： CB-1调节化合物及其用途
公开(公告)号：WO2007047737A1
公开(公告)日：2007-04-26
申请号：PCT/US2006/040662
申请日：2006-10-17
申请人： ACADIA PHARMACEUTICALS INC. , OLSSON, Roger , EK, Fredrik , OTTESEN, Lars, Korsgaard , BULOW, Anne
发明人： OLSSON, Roger , EK, Fredrik , OTTESEN, Lars, Korsgaard , BULOW, Anne
IPC分类号： C07D419/12 , C07D267/20 , C07D245/06 , C07D225/08 , C07D295/18 , C07D337/14 , C07D281/16 , C07F7/08 , C07D419/04 , C07D417/04 , A61P25/00 , A61K31/5513 , A61K31/554 , A61K31/551
CPC分类号： C07D419/12 , C07D223/20 , C07D225/08 , C07D243/38 , C07D245/06 , C07D267/20 , C07D281/16 , C07D295/192 , C07D337/14 , C07D417/04 , C07D417/06 , C07D417/12 , C07D417/14 , C07D419/04
摘要： Disclosed herein is a compound of Formula (I). Also disclosed herein is a method of modulating the activity of a cannabinoid receptor using a compound of Formula (I). Furthermore, disclosed herein is a method of treating a disease or condition that would be alleviated, improved or prevented by administration of a compound that modulates a cannabinoid receptor comprising identifying a subject in need thereof and administering to said subject a therapeutically effective amount of a compound of Formula (I). Also disclosed herein are pharmaceutical compositions comprising a compound of Formula (I).
摘要翻译：本文公开了式（I）的化合物。本文还公开了使用式（I）的化合物调节大麻素受体的活性的方法。此外，本文公开的是治疗可以通过施用调节大麻素受体的化合物减轻，改善或预防的疾病或病症的方法，包括鉴定有需要的受试者，并向所述受试者施用治疗有效量的化合物的式（I）。本文还公开了包含式（I）化合物的药物组合物。

5. 发明申请

WO2023083895A1 HYDROPHILIC AZADIBENZOCYCLOOCTYNE DERIVATIVES AND METAL-FREE CLICK REACTIONS WITH THESE HYDROPHILIC AZADIBENZOCYCLOOCTYNE DERIVATIVES 审中-公开
公开(公告)号：WO2023083895A1
公开(公告)日：2023-05-19
申请号：PCT/EP2022/081339
申请日：2022-11-09
申请人： F. HOFFMANN-LA ROCHE AG , ROCHE DIAGNOSTICS GMBH , ROCHE DIAGNOSTICS OPERATIONS, INC.
发明人： BERGMANN, Frank , HEINDL, Dieter , WINTER, Nils
IPC分类号： C07D225/08 , A61K47/50
摘要： The invention relates in a first aspect to an azadibenzocyclooctyne derivative according to formula (I) or a salt thereof having specific substituents at the benzo rings of the DIBAC structure and having specific substituents connected to the nitrogen atom of the DIBAC structure. A second aspect of the invention is directed to a conjugate of formula (II), wherein a substituent R6 is connected to the N atom of the 8 membered ring of the DIBAC structure via a linker structure –C(=O)-[L]n-Z-. A third aspect of the invention relates to a method for the modification of a target molecule, wherein a conjugate according to the second aspect is reacted with a target molecule comprising a 1,3-dipole group or a 1,3-(hetero)diene group. In a fourth aspect, the invention is directed to the use of the conjugate according to the second aspect for bioorthogonal labeling and/or modification of a target molecule. A fifth aspect of the invention relates to a modified target molecule comprising the reaction product of a conjugate according to the second aspect and a target molecule comprising a 1,3-dipole group or a 1,3-(hetero)diene group, obtained or obtainable from the method of the third aspect. In a sixth aspect, the invention is related to a kit comprising a modified target molecule according to the fifth aspect as detector reagent and a suitable capture reagent.

6. 发明申请

WO2012047663A3 METHODS INCLUDING LATENT 1,3-DIPOLE-FUNCTIONAL COMPOUNDS AND MATERIALS PREPARED THEREBY 审中-公开
公开(公告)号：WO2012047663A3
公开(公告)日：2012-04-12
申请号：PCT/US2011/053487
申请日：2011-09-27
申请人： UNIVERSITY OF GEORGIA REASERCH FOUNDATION, INC. , BOONS, Geert-Jan , FRISCOURT, Frédéric , LEDIN, Petr A. , MBUA, Ngalle Eric
发明人： BOONS, Geert-Jan , FRISCOURT, Frédéric , LEDIN, Petr A. , MBUA, Ngalle Eric
IPC分类号： C07D225/08 , C07D261/20 , C07D413/06 , C07D249/16
摘要： Methods that include latent 1,3-dipole-functional compounds are disclosed herein. The latent 1,3-dipole-functional compound (e.g., an oxime) can be used to form an active 1,3-dipole-functional compound (e.g., a nitrile oxide) that can be used to react with a cyclic alkyne in a dipolar cycloaddition reaction.

7. 发明申请

WO2008055068A3 INHIBITORS OF HISTONE DEACETYLASE 审中-公开
标题翻译： HISTONE DEACETYLASE的抑制剂
公开(公告)号：WO2008055068A3
公开(公告)日：2009-03-05
申请号：PCT/US2007082668
申请日：2007-10-26
申请人： METHYGENE INC , EN VIVO PHARMACEUTICALS INC , DEZIEL ROBERT , LEIT SILVANA , BEAULIEU PATRICK , CHANTIGNY YVES ANDRE , MANCUSO JOHN , TESSIER PIERRE , SHAPIRO GIDEON , CHESWORTH RICHARD , SMIL DAVID
发明人： DEZIEL ROBERT , LEIT SILVANA , BEAULIEU PATRICK , CHANTIGNY YVES ANDRE , MANCUSO JOHN , TESSIER PIERRE , SHAPIRO GIDEON , CHESWORTH RICHARD , SMIL DAVID
IPC分类号： C07D209/22 , A61K31/55 , A61K31/5513 , A61K31/553 , A61K31/554 , A61P43/00 , C07D209/70 , C07D221/12 , C07D223/26 , C07D225/08 , C07D239/28 , C07D239/34 , C07D239/42 , C07D243/14 , C07D243/24
CPC分类号： C07D498/04 , C07C259/06 , C07C259/10 , C07D209/02 , C07D209/08 , C07D209/52 , C07D209/94 , C07D221/12 , C07D223/16 , C07D223/20 , C07D223/22 , C07D223/24 , C07D223/26 , C07D223/28 , C07D225/08 , C07D239/28 , C07D239/34 , C07D239/42 , C07D243/24 , C07D243/38 , C07D265/38 , C07D267/14 , C07D267/18 , C07D267/20 , C07D279/22 , C07D279/26 , C07D281/16 , C07D285/36 , C07D291/08 , C07D295/155 , C07D313/12 , C07D401/14 , C07D403/04 , C07D403/14 , C07D413/06 , C07D413/12 , C07D471/04 , C07D471/08 , C07D471/14 , C07D487/04 , C07D487/08 , C07D487/14 , C07D491/08 , C07D495/04 , C07D513/04 , C07H13/10
摘要： This invention relates to compounds for the inhibition of histone deacetylase. More particularly, the invention provides for compounds of formula (I) wherein (B), Q, J, L and Z are as defined in the specification.
摘要翻译：本发明涉及抑制组蛋白脱乙酰酶的化合物。更具体地，本发明提供式（I）的化合物，其中（B），Q，J，L和Z如说明书中所定义。

8. 发明申请

WO99037619A1 CHEMOKINE RECEPTOR ANTAGONISTS AND METHODS OF USE THEREFOR 审中-公开
标题翻译：化疗受体拮抗剂及其使用方法
公开(公告)号：WO99037619A1
公开(公告)日：1999-07-29
申请号：PCT/US1999/001367
申请日：1999-01-21
IPC分类号： A61K31/438 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/445 , A61K31/451 , A61K31/4523 , A61K31/4525 , A61K31/4535 , A61K31/4545 , A61K31/5377 , A61K31/55 , A61P1/00 , A61P1/04 , A61P3/10 , A61P9/00 , A61P9/10 , A61P11/06 , A61P17/06 , A61P19/02 , A61P25/00 , A61P29/00 , A61P37/06 , A61P37/08 , A61P43/00 , C07D211/52 , C07D223/20 , C07D313/12 , C07D337/12 , C07D401/06 , C07D401/14 , C07D405/06 , C07D409/06 , C07D409/14 , C07D487/04 , C07D491/04 , C07D491/044 , C07D493/04 , C07D495/04 , C07D495/10 , C07D519/00 , C07D221/16 , C07D225/08 , C07D313/10
CPC分类号： C07D405/06 , A61K31/451 , A61K31/4523 , A61K31/4525 , A61K31/4535 , A61K31/4545 , A61K31/5377 , A61K31/55 , C07D211/52 , C07D313/12 , C07D337/12 , C07D409/06 , C07D409/14 , C07D491/04 , C07D493/04
摘要： Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to a subject in need an effective amount of a compound represented by structural formula (I) and physiologically acceptable salts thereof.
摘要翻译：公开了新型化合物和治疗与异常白细胞募集和/或激活相关的疾病的方法。该方法包括向有需要的受试者施用有效量的由结构式（I）表示的化合物及其生理学上可接受的盐。

9. 发明申请

WO99020599A1 PHARMACEUTICALLY ACTIVE COMPOUNDS AND METHODS OF USE 审中-公开
标题翻译：药物活性化合物及其使用方法
公开(公告)号：WO99020599A1
公开(公告)日：1999-04-29
申请号：PCT/US1998/022309
申请日：1998-10-20
IPC分类号： C07D243/12 , A61K31/155 , A61K31/381 , A61K31/403 , A61K31/4035 , A61K31/404 , A61K31/4045 , A61K31/4402 , A61K31/4406 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/473 , A61K31/55 , A61K31/5513 , A61P1/08 , A61P9/02 , A61P9/10 , A61P25/06 , A61P25/28 , A61P25/32 , A61P31/04 , C07C279/22 , C07C323/44 , C07D209/08 , C07D209/16 , C07D209/44 , C07D209/90 , C07D213/81 , C07D213/82 , C07D215/06 , C07D217/04 , C07D221/10 , C07D221/12 , C07D223/16 , C07D223/22 , C07D223/24 , C07D225/08 , C07D233/90 , C07D245/06 , C07D277/30 , C07D307/68 , C07D333/24 , C07D333/38 , C07D401/12 , C07D405/12 , C07D409/12 , C07C233/00 , C07C235/00 , C07C237/00 , C07D207/08 , C07D207/30 , C07D207/46 , C07D209/18 , C07D211/30 , C07D211/32 , C07D215/38 , C07D233/66 , C07D239/02 , C07D241/00 , C07D241/02 , C07D249/04 , C07D249/08 , C07D249/14 , C07D261/06 , C07D263/34 , C07D265/30 , C07D271/06 , C07D271/10 , C07D271/12 , C07D275/02 , C07D295/18 , C07D307/02 , C07D307/78 , C07D307/87 , C07D307/93 , C07D311/02 , C07D315/00 , C07D333/22 , C07D333/56 , C07D333/72 , C07D403/00 , C07D409/02 , C07D413/00 , C07D417/00 , C07D487/00 , C07D498/00 , C07D513/00
CPC分类号： C07D223/16 , C07C279/22 , C07C323/44 , C07C2601/14 , C07C2603/74 , C07D209/08 , C07D209/16 , C07D209/90 , C07D215/06 , C07D217/04 , C07D221/10 , C07D223/24 , C07D225/08 , C07D333/24
摘要： The present invention relates to pharmaceutically acceptable compounds, including acylguanidine compounds, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are particularly useful for the treatment or prophylaxis of neurological injury and neurodegenerative disorders.
摘要翻译：本发明涉及药学上可接受的化合物，包括酰基胍化合物，以及使用或包含一种或多种这些化合物的治疗方法和药物组合物。本发明的化合物特别可用于治疗或预防神经损伤和神经变性疾病。

10. 发明申请

WO98051298A1 ARYLSUBSTITUTED PIPERAZINES USEFUL IN THE TREATEMENT OF BENIGN PROSTATIC HYPERLASIA 审中-公开
标题翻译：用于治疗预防性高血压的ARYLSUTITUTED PIPERAZINES
公开(公告)号：WO98051298A1
公开(公告)日：1998-11-19
申请号：PCT/US1998/009023
申请日：1998-05-08
IPC分类号： C07D295/12 , A61K31/397 , A61K31/40 , A61K31/4015 , A61K31/402 , A61K31/4025 , A61K31/445 , A61K31/496 , A61K31/55 , A61P13/08 , C07D205/08 , C07D207/12 , C07D207/26 , C07D207/27 , C07D207/28 , C07D209/44 , C07D209/48 , C07D211/40 , C07D211/76 , C07D221/20 , C07D223/10 , C07D225/02 , C07D225/08 , C07D241/04 , C07D295/08 , C07D295/13 , C07D401/12 , C07D403/12 , A61K31/33 , A61K31/395 , A61K31/495
CPC分类号： C07D207/27 , C07D207/28 , C07D209/48 , C07D211/76 , C07D223/10 , C07D295/13
摘要： This invention relates to a series of arylsubstituted piperazines, of Formula (I), pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention selectively inhibit binding to the alpha -1a adrenergic receptor, a receptor which has been implicated in benign prostatic hyperplasia. As such the compounds are potentially useful in the treatment of this and other disease.
摘要翻译：本发明涉及式（I）的一系列芳基取代哌嗪，含有它们的药物组合物和用于其制备的中间体。本发明的化合物选择性地抑制与α-1肾上腺素能受体的结合，α受体是牵涉到良性前列腺增生的受体。因此，这些化合物在治疗这种和其它疾病中潜在有用。

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