-
公开(公告)号:WO2022206666A1
公开(公告)日:2022-10-06
申请号:PCT/CN2022/083323
申请日:2022-03-28
申请人: 广东东阳光药业有限公司
IPC分类号: C07D207/325 , C07D207/34 , A61K31/40 , A61P9/00 , A61P9/04 , A61P9/10 , A61P9/12 , A61P13/12
摘要: 提供一种吡咯酰胺化合物的晶型及其制备方法和用途,还提供了包含所述晶型的药物组合物。具体地,所述晶型或所述药物组合物可用于治疗和预防醛甾酮过多症、糖尿病肾病、高血压、心力衰竭(包括慢性心力衰竭等)、心肌梗死的后遗症、肝硬化、肾衰竭和中风等疾病。
-
公开(公告)号:WO2020161148A3
公开(公告)日:2020-08-13
申请号:PCT/EP2020/052782
申请日:2020-02-04
IPC分类号: C07D207/325 , C07D207/337 , C07D207/34 , C07D403/04
摘要: The present invention relates to pyrazole derivatives of formula (X) wherein ring A is a pyrazole and substituents R B1 , R B2 , n, R Q1 , R Q2 , R Q3 , and R Q4 are as defined in claim 1, their manufacture, and their use in the manufacture of agrochemicals and pharmaceuticals.
-
公开(公告)号:WO2011079007A1
公开(公告)日:2011-06-30
申请号:PCT/US2010/060671
申请日:2010-12-16
申请人: IRONWOOD PHARMACEUTICALS, INC. , MERMERIAN, Ara , PENG, Bo , HUDSON, Colleen , KIM, Charles , MOORE, Joel , ROHDE, Jason , SPROTT, Kevin , GRAUL, Regina , NAKAI, Takashi , JIA, James , BARTOLINI, Wilmin
发明人: MERMERIAN, Ara , PENG, Bo , HUDSON, Colleen , KIM, Charles , MOORE, Joel , ROHDE, Jason , SPROTT, Kevin , GRAUL, Regina , NAKAI, Takashi , JIA, James , BARTOLINI, Wilmin
IPC分类号: C07D401/04 , C07D403/12 , C07D413/14 , C07D207/325 , A61K31/40 , A61K31/495 , A61P43/00
CPC分类号: C07D403/12 , C07D207/325 , C07D401/04 , C07D413/14
摘要: Modulators of CRTH2, particularly antagonists of CRTH2, that are useful for treating various disorders, including asthma and respiratory disorders are disclosed. The compounds fall within a genus described by formula I.
摘要翻译: 公开了可用于治疗各种疾病(包括哮喘和呼吸系统疾病)的CRTH2调节剂,特别是CRTH2拮抗剂。 化合物属于式I所述的一类。
-
公开(公告)号:WO2009157418A1
公开(公告)日:2009-12-30
申请号:PCT/JP2009/061350
申请日:2009-06-23
IPC分类号: C07C59/66 , A61K31/192 , A61K31/195 , A61K31/196 , A61K31/275 , A61K31/343 , A61K31/40 , A61K31/4192 , A61K31/426 , A61K31/428 , A61K31/47 , A61K31/4741 , A61P1/14 , A61P3/04 , A61P3/06 , A61P3/10 , A61P7/02 , A61P7/10 , A61P9/10 , A61P9/12 , A61P15/00 , A61P17/00 , A61P19/02 , A61P19/08 , A61P25/28 , A61P35/00 , C07C205/34 , C07C217/76 , C07C229/42 , C07C255/54 , C07C311/29 , C07C317/22 , C07D207/325 , C07D215/22 , C07D249/04 , C07D277/24 , C07D277/64 , C07D307/83 , C07D491/048
CPC分类号: C07D207/325 , A61K31/192 , A61K31/195 , A61K31/196 , A61K31/275 , A61K31/343 , A61K31/40 , A61K31/4192 , A61K31/426 , A61K31/428 , A61K31/47 , A61K31/4741 , C07C59/66 , C07C59/72 , C07C205/34 , C07C205/37 , C07C217/76 , C07C229/42 , C07C255/54 , C07C311/29 , C07C317/22 , C07C2601/02 , C07C2602/08 , C07D215/22 , C07D249/04 , C07D277/24 , C07D277/64 , C07D307/83 , C07D491/048
摘要: 優れた活性及び安全性を有する糖尿病等の治療薬及び/又は予防薬を見出すこと。 下記一般式(I) [式中、Xは=C(R5)-又は=N-、Yは-O-又は-NH-、Lは単結合又は置換可C1-C3アルキレン基、Mは置換可C3-C10シクロアルキル基、置換可C6-C10アリール基又は置換可複素環基、R 1 はC1-C6アルキル基、C3-10シクロアルキル基、C1-C6ハロアルキル基、C1-C6アルケニル基、C1-C6アルキニル基、C1-C6脂肪族アシル基、C1-C6アルコキシC1-C6アルキル基又はC6-C10アリール基、R 2 、R 3 、R 4 及びR 5 はそれぞれ同一若しくは異なって、水素原子、ハロゲン原子、C1-C3アルキル基、C1-C3ハロアルキル基、C1-C3アルコキシ基又はニトロ基を示す。ただし、上記R 1 とR 2 のアルキル基部分が結合し、酸素原子を1個含む5-6員複素環を形成していてもよい。] で表される化合物又はその薬理上許容される塩。
摘要翻译: 公开了用于治疗和/或预防糖尿病等的高度安全的药剂,其具有优异的活性。 具体公开的是由通式(I)表示的化合物或其药理学上可接受的盐。 (式中,X表示= C(R5) - 或= N-; Y表示-O-或-NH-; L表示单键或任意取代的C1-C3亚烷基; M表示任意取代的C3- C10环烷基,任选取代的C 6 -C 10芳基或任选取代的杂环基; R 1表示C 1 -C 6烷基,C 3 -C 10环烷基,C 1 -C 6卤代烷基,C 1 -C 6链烯基, C1-C6炔基,C1-C6脂族酰基,C1-C6烷氧基C1-C6烷基或C6-C10芳基; R2,R3,R4和R5可以相同或不同,表示 氢原子,卤素原子,C1-C3烷基,C1-C3卤代烷基,C1-C3烷氧基或硝基,这时R1和R2的烷基部分可以各自键合 另外形成含有一个氧原子的5-或6-元杂环)
-
公开(公告)号:WO2009079683A1
公开(公告)日:2009-07-02
申请号:PCT/AU2008/001781
申请日:2008-12-02
申请人: THE UNIVERSITY OF SYDNEY , KASSIOU, Michael , JAMES, Michelle, Louise , LUUS, Christopher, Andrew
IPC分类号: C07D471/04 , A61P25/08 , A61P35/00 , A61K31/402 , A61P25/16 , C07D207/325 , A61K31/437 , A61P25/22 , C07D401/04 , A61K31/4439 , A61P25/24 , A61K101/02 , A61K49/00 , A61P25/28 , A61K51/04 , A61P29/00
CPC分类号: C07D487/04 , A61K51/0446 , A61K51/0455 , A61K51/0459 , C07D207/325 , C07D207/337 , C07D401/04
摘要: The present invention relates to compounds and methods for imaging translocator protein (18 kDa) (TSPO) expression in a subject. This invention also relates to compounds and methods for the treatment of neurodegenerative disorders, inflammation or anxiety in a subject.
摘要翻译: 本发明涉及在受试者中成像易位蛋白(18kDa)(TSPO)表达的化合物和方法。 本发明还涉及用于治疗受试者的神经变性疾病,炎症或焦虑症的化合物和方法。
-
公开(公告)号:WO2004039795A3
公开(公告)日:2005-03-24
申请号:PCT/JP0313683
申请日:2003-10-27
申请人: FUJISAWA PHARMACEUTICAL CO , DAISO CO LTD , INOUE YOSHIKAZU , TERASAWA TAKESHI , TAKASUGI HISASHI , NAGAYOSHI AKIRA , UESHIMA KOJI , SAWADA MASAE , FURUKAWA YOSHIRO , MIKAMI MASAFUMI , HINOUE KAZUMASA , FUKUMOTO DAISUKE
发明人: INOUE YOSHIKAZU , TERASAWA TAKESHI , TAKASUGI HISASHI , NAGAYOSHI AKIRA , UESHIMA KOJI , SAWADA MASAE , FURUKAWA YOSHIRO , MIKAMI MASAFUMI , HINOUE KAZUMASA , FUKUMOTO DAISUKE
IPC分类号: A61P3/06 , C07D207/32 , C07D207/325 , C07D209/08 , C07D213/30 , C07D213/38 , C07D213/40 , C07D213/56 , C07D213/73 , C07D213/74 , C07D213/75 , C07D213/81 , C07D213/82 , C07D217/22 , C07D231/12 , C07D231/38 , C07D249/08 , C07D277/40 , C07D277/48 , C07D295/155 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D417/12 , C07D417/14
CPC分类号: C07D207/325 , C07D209/08 , C07D213/30 , C07D213/38 , C07D213/40 , C07D213/56 , C07D213/73 , C07D213/74 , C07D213/75 , C07D213/81 , C07D213/82 , C07D217/22 , C07D231/12 , C07D231/38 , C07D249/08 , C07D277/40 , C07D277/48 , C07D295/155 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D417/12 , C07D417/14
摘要: A compound of the formula (I) Wherein R is hydrogen, lower alkyl, lower alkenyl, halo(lower)alkyl, cyclo(lower)alkyl, lower alkoxy, lower alkylthio, acyl, optionally substituted aryl or NR R ; R is hydrogen; or aryl or heteroaryl, each of which may be substituted; X is direct bond or bivalent residue derived from piperazine; Y is -(A )n-(A )m-, wherein n and m are independently 0 or 1) ; (II) is bivalent residue derived from arene or heteroarene; and (III) is bivalent residue derived from arene or heteroarene, or a salt thereof. The compound of the present invention and a salt thereof inhibit apolipoprotein B (Apo B) secretion and are useful as a medicament for prophylactic and treatment of diseases or conditions resulting from elevated circulating levels of Apo B.
摘要翻译: 式(I)的化合物,其中R 1是氢,低级烷基,低级烯基,卤代(低级)烷基,环(低级)烷基,低级烷氧基,低级烷硫基,酰基,任选取代的芳基或NR 3 [R <4>; R 2是氢; 或芳基或杂芳基,其各自可以被取代; X是衍生自哌嗪的直接键或二价残基; Y是 - (A 1)n - (A 2)m - ,其中n和m独立地为0或1); (II)是衍生自芳烃或杂芳烃的二价残基; 和(III)是衍生自芳烃或杂芳烃的二价残基或其盐。 本发明化合物及其盐抑制载脂蛋白B(Apo B)分泌,可用作预防和治疗由ApoB升高的循环水平引起的疾病或病症的药物。
-
7.2-SUBSTITUTED-3-PROPENAMIDE DERIVATIVES AND METHODS OF USING THE SAME 审中-公开
标题翻译: 2-取代-3-丙酰胺衍生物及其使用方法公开(公告)号:WO2004050613A3
公开(公告)日:2004-09-23
申请号:PCT/US0338233
申请日:2003-12-02
申请人: GILEAD SCIENCES INC , SZNAIDMAN MARCOS , PAINTER GEORGE R , ALMOND MERRICK R , CLEARY DARRYL G , PESYAN AMIR
IPC分类号: C07C235/38 , C07C237/22 , C07D203/18 , C07D205/04 , C07D207/20 , C07D207/24 , C07D207/32 , C07D207/325 , C07D207/33 , C07D211/18 , C07D211/58 , C07D211/62 , C07D211/70 , C07D213/26 , C07D213/40 , C07D213/75 , C07D213/82 , C07D231/40 , C07D233/06 , C07D233/54 , C07D239/06 , C07D239/26 , C07D239/42 , C07D239/48 , C07D239/52 , C07D241/20 , C07D251/22 , C07D253/07 , C07D261/14 , C07D263/12 , C07D277/04 , C07D277/22 , C07D277/46 , C07D277/58 , C07D285/12 , C07D285/135 , C07D295/185 , C07D295/205 , C07D307/10 , C07D307/14 , C07D307/20 , C07D307/38 , C07D307/52 , C07D307/56 , C07D307/79 , C07D309/04 , C07D309/20 , C07D317/46 , C07D317/52 , C07D317/62 , C07D317/64 , C07D319/18 , C07D333/12 , C07D333/20 , C07D333/36 , C07D333/44 , C07D401/12 , C07D405/12 , C07D417/12 , C07D491/10 , C07D211/60 , A61K31/445 , C07D211/98 , C07D401/00
CPC分类号: C07D207/325 , C07C235/38 , C07C237/22 , C07D203/18 , C07D205/04 , C07D207/20 , C07D207/24 , C07D207/33 , C07D211/18 , C07D211/58 , C07D211/62 , C07D211/70 , C07D213/26 , C07D213/40 , C07D213/75 , C07D213/82 , C07D231/40 , C07D233/06 , C07D233/64 , C07D239/06 , C07D239/26 , C07D239/42 , C07D239/48 , C07D239/52 , C07D241/20 , C07D251/22 , C07D253/07 , C07D261/14 , C07D263/12 , C07D277/04 , C07D277/22 , C07D277/46 , C07D277/58 , C07D285/135 , C07D295/185 , C07D295/205 , C07D307/10 , C07D307/14 , C07D307/20 , C07D307/38 , C07D307/52 , C07D307/56 , C07D307/79 , C07D309/04 , C07D309/20 , C07D317/46 , C07D317/52 , C07D317/62 , C07D317/64 , C07D319/18 , C07D333/12 , C07D333/20 , C07D333/36 , C07D333/44 , C07D401/12 , C07D405/12 , C07D417/12 , C07D491/10
摘要: This invention provides 2-substituted-propenamide derivatives and their compositions for the treament of hepatitis B virus and/or hepatitis D virus.
摘要翻译: 本发明提供了用于治疗乙型肝炎病毒和/或丁型肝炎病毒的2-取代丙烯酰胺衍生物及其组合物。
-
8.4-(3,3-DIHALO-ALLYLOXY) PHENOL DERIVATIVES HAVING PESTICIDAL PROPERTIES 审中-公开
标题翻译: 具有农药性质的4-(3,3-DIHALO-ALLYLOXY)苯酚衍生物公开(公告)号:WO2004020445A3
公开(公告)日:2004-04-15
申请号:PCT/EP0309636
申请日:2003-08-29
申请人: SYNGENTA PARTICIPATIONS AG , ZAMBACH WERNER , STEIGER ARTHUR , RENOLD PETER , TRAH STEPHAN , HALL ROGER GRAHAM
IPC分类号: A01N43/36 , A01N43/56 , A01N43/653 , A01N43/713 , A01N43/76 , A01N43/78 , A01N43/80 , A01N43/82 , A01N43/90 , A01N47/18 , A01N47/20 , C07D207/32 , C07D207/325 , C07D207/333 , C07D207/34 , C07D231/12 , C07D231/22 , C07D231/38 , C07D249/08 , C07D249/10 , C07D257/04 , C07D261/08 , C07D261/10 , C07D261/18 , C07D263/32 , C07D263/34 , C07D271/06 , C07D271/07 , C07D277/24 , C07D277/30 , C07D277/40 , C07D277/48 , C07D277/56 , C07D285/08 , C07D285/12 , C07D333/16 , C07D333/38 , C07D471/04
CPC分类号: C07D207/325 , A01N43/36 , A01N43/56 , A01N43/653 , A01N43/713 , A01N43/76 , A01N43/78 , A01N43/80 , A01N43/82 , A01N43/90 , A01N47/18 , A01N47/20 , C07D207/333 , C07D207/34 , C07D231/12 , C07D231/22 , C07D231/38 , C07D249/08 , C07D249/10 , C07D257/04 , C07D261/08 , C07D261/10 , C07D261/18 , C07D263/32 , C07D263/34 , C07D271/06 , C07D271/07 , C07D277/24 , C07D277/30 , C07D277/40 , C07D277/48 , C07D277/56 , C07D285/08 , C07D285/12 , C07D333/16 , C07D333/38 , C07D471/04
摘要: Compounds of formula (I) wherein Ao is a bond or a C1-C6alkylene bridge; A1, A2 and A3 are a C1-C6alkylene bridge; D is CH or N; W is, for example, O, S, SO, S02, -C(=O)-O- or -O-C(=O)-; T is a bond or, for example, O, NH, S, SO or SR2; Q is, for example, O, S, SO or SO2; Y is, for example, O, S, SO or SO2; X1 and X2 are each independently of the other fluorine, chlorine or bromine; R1, R2 and R3 are, for example, H, halogen, OH, SH, CN or nitro; R4 is, for example, H, halogen, OH, SH, CN, nitro or C1-C6alkyl; R5 is, for example, H, CN, OH, C1-C6alkyl or C3-C8cycloalkyl; k is 1, 2 or 3 when D is nitrogen; or is 1, 2, 3 or 4 when D is CH; m is 1 or 2; E is heteroaryl which is unsubstituted or substituted - depending upon the substitutions possible on the ring - by from one to four identical or different substituents selected from R10; and R10 is, for example, halogen, CN, NO2, OH, SH or C1-C6alkyl; and, where applicable, their possible E/Z isomers, E/Z isomeric mixtures and/or tautomers, in each case in free form or in salt form, a process for the preparation of those compounds and their use, pesticidal compositions in which the active ingredient has been selected from those compounds or an agrochemically acceptable salt thereof, a process for the preparation of those compositions and their use, plant propagation material treated with those compositions, and a method of controlling pests.
摘要翻译: 式(I)的化合物,其中Ao是一个键或C1-C6亚烷基桥; A1,A2和A3是C1-C6亚烷基桥; D是CH或N; W是例如O,S,SO,SO 2,-C(= O)-O-或-O-C(= O) - ; T是键或例如O,NH,S,SO或SR2; Q是例如O,S,SO或SO 2; Y是例如O,S,SO或SO 2; X1和X2各自独立地为氟,氯或溴; R1,R2和R3是例如H,卤素,OH,SH,CN或硝基; R4是例如H,卤素,OH,SH,CN,硝基或C1-C6烷基; R5是例如H,CN,OH,C1-C6烷基或C3-C8环烷基; 当D为氮时,k为1,2或3; 或当D为CH时为1,2,3或4; m为1或2; E是未取代或取代的杂芳基 - 取决于环上可能的取代基 - 通过一至四个相同或不同的选自R 10的取代基; R 10为例如卤素,CN,NO 2,OH,SH或C 1 -C 6烷基; 在适用情况下,它们可能的E / Z异构体,E / Z异构体混合物和/或互变异构体,在每种情况下为游离形式或盐形式,制备这些化合物及其用途的方法,其中 从这些化合物或其农业化学上可接受的盐中选择活性成分,制备这些组合物的方法及其用途,用这些组合物处理的植物繁殖材料以及防治害虫的方法。
-
公开(公告)号:WO03027061A3
公开(公告)日:2003-07-31
申请号:PCT/US0225969
申请日:2002-09-09
申请人: LILLY CO ELI , ALLEN JENNIFER REBECCA , HITCHCOCK STEPHEN ANDREW , LIU BIN , TURNER WILLIAM WILSON JR , JAMISON JAMES ANDREW
发明人: ALLEN JENNIFER REBECCA , HITCHCOCK STEPHEN ANDREW , LIU BIN , TURNER WILLIAM WILSON JR , JAMISON JAMES ANDREW
IPC分类号: C07D333/38 , A61K31/166 , A61K31/341 , A61K31/381 , A61K31/44 , A61K31/4436 , A61K31/4965 , A61P25/18 , A61P25/28 , A61P43/00 , C07C257/14 , C07D207/32 , C07D207/325 , C07D213/54 , C07D213/56 , C07D213/81 , C07D213/82 , C07D213/84 , C07D241/24 , C07D307/52 , C07D317/28 , C07D333/24 , C07D409/04 , C07C251/00
CPC分类号: C07D207/325 , C07C257/14 , C07C2602/08 , C07D213/54 , C07D213/56 , C07D213/81 , C07D213/82 , C07D213/84 , C07D241/24 , C07D307/52 , C07D317/28 , C07D333/24 , C07D409/04 , Y02P20/582
摘要: The present invention relates to compounds of Formula I: Formula I which are agonists of the M-1 muscarinic receptor.
摘要翻译: 本发明涉及作为M-1毒蕈碱受体的激动剂的式I化合物:式I。
-
公开(公告)号:WO0212214A3
公开(公告)日:2002-06-20
申请号:PCT/US0124655
申请日:2001-08-06
发明人: APODACA RICHARD , CARRUTHERS NICHOLAS I , DVORAK CURT A , RUDOLPH DALE A , SHAH CHANDRAVADAN R , XIAO WEI
IPC分类号: C07D295/08 , A61K31/4402 , A61K31/4439 , A61K31/4453 , A61K31/4465 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/4725 , A61K31/495 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K45/00 , A61K45/06 , A61K51/00 , A61P9/00 , A61P11/00 , A61P11/06 , A61P25/00 , A61P25/06 , A61P25/08 , A61P25/20 , A61P25/24 , A61P25/28 , A61P27/16 , A61P37/08 , A61P43/00 , C07C217/22 , C07C323/25 , C07C335/32 , C07D207/09 , C07D207/32 , C07D207/325 , C07D207/335 , C07D211/14 , C07D211/22 , C07D211/46 , C07D211/52 , C07D211/58 , C07D211/62 , C07D211/70 , C07D213/36 , C07D213/74 , C07D215/06 , C07D217/04 , C07D233/42 , C07D233/54 , C07D233/84 , C07D233/88 , C07D235/06 , C07D235/26 , C07D239/34 , C07D257/04 , C07D277/36 , C07D295/092 , C07D295/096 , C07D295/112 , C07D295/135 , C07D295/20 , C07D295/205 , C07D307/52 , C07D317/28 , C07D333/20 , C07D401/04 , C07D401/12 , C07D401/14 , C07D471/08 , C07D487/08 , C07D491/113 , C07D521/00 , A61K31/357 , A61K31/40 , A61K31/403 , A61K31/4184 , A61K31/4427 , A61K31/47 , A61K31/505 , C07D209/08 , C07D295/088
CPC分类号: C07D207/325 , A61K31/4402 , A61K31/4465 , A61K45/06 , C07C217/22 , C07C323/25 , C07C335/32 , C07D207/335 , C07D211/22 , C07D211/46 , C07D211/58 , C07D213/36 , C07D213/74 , C07D215/06 , C07D231/12 , C07D233/42 , C07D233/54 , C07D233/56 , C07D233/84 , C07D233/88 , C07D235/06 , C07D235/26 , C07D239/34 , C07D249/08 , C07D257/04 , C07D277/36 , C07D295/088 , C07D295/096 , C07D295/112 , C07D295/135 , C07D295/205 , C07D307/52 , C07D317/28 , C07D333/20 , C07D401/04 , C07D401/12 , C07D401/14 , C07D471/08 , A61K2300/00
摘要: Substituted aryloxyalkylamines of formula (I), compositions containing them, and methods of making and using them to treat histamine-mediated conditions.
摘要翻译: 式(I)的取代的芳氧基烷基胺,含有它们的组合物,以及制备和使用它们来治疗组胺介导的病症的方法。
-
-
-
-
-
-
-
-
-