公开(公告)号：EP3307732A1

公开(公告)日：2018-04-18

申请号：EP16730222.3

申请日：2016-06-10

申请人： Biogen MA Inc.

发明人： MACPHEE, J. Michael ,  HUMORA, Michael

IPC分类号： C07D403/14 ,  A61K31/506 ,  A61P35/00 ,  A61P37/00

CPC分类号： C07D403/14 ,  C07B2200/13 ,  C07C55/07 ,  C07C55/08 ,  C07C55/10 ,  C07C55/28 ,  C07C57/145 ,  C07C57/15 ,  C07C57/44 ,  C07C59/11 ,  C07C59/245 ,  C07C59/255 ,  C07C59/265 ,  C07C229/22 ,  C07C229/24 ,  C07C229/26 ,  C07C229/36 ,  C07C233/83 ,  C07C237/12 ,  C07C309/04 ,  C07C309/05 ,  C07C309/08 ,  C07C309/29 ,  C07C309/30 ,  C07C309/35 ,  C07D207/16 ,  C07D207/28 ,  C07D213/80 ,  C07D213/82 ,  C07D275/06

摘要： The present invention provides compounds and compositions thereof which are useful as inhibitors of Bruton's tyrosine kinase and which exhibit desirable characteristics for the same.

公开(公告)号：EP0130482A1

公开(公告)日：1985-01-09

申请号：EP84107104.6

申请日：1984-06-20

申请人： Research Corporation

发明人： Brown, Davis B. ,  Khokhar, Abdul R. ,  Hacker, Miles P. ,  McCommack, John J.

IPC分类号： C07C87/38 ,  A61K31/28 ,  C07D307/00 ,  C07D205/04 ,  C07H23/00 ,  C07C61/00 ,  C07C62/32 ,  C07C101/00 ,  C07C143/08 ,  C07C147/00 ,  C07C161/00

CPC分类号： C07C309/00 ,  C07C51/418 ,  C07C55/28 ,  C07C59/105 ,  C07C61/04 ,  C07C61/06 ,  C07C61/08 ,  C07C61/09 ,  C07C61/20 ,  C07C61/22 ,  C07F15/0093

摘要： Diaminocyclohexane platinum complexes having the structural formula
or
wherein: X is a monovalent anion selected from the group consisting of ascorbate, isoascorbate, monosaccharate, saccharate-4-lactone, shikimate, isethionate, 2-aminoethylsulfate, azetidinecarboxylate, proline, hydroxyproline, pipecolinate, cyclopropanecarboxylate, cyclobutanecarboxylate, cyclopentanecarboxylate, cyclopentenecarboxylate, cyclohexanecarboxylate, cyclohexenecarboxylate, bicine, glycine, 2-aminoethanesulfonate, 2-chloroethanesulfonate and
Y is a divalent anion selected from the group consisting of iminodiacetate, isocitratelactone, furanedicarboxylate, cyclopropane-1,1-dicarboxylate, isocitratomonoethylester, N-methyliminodiacetate, N-(2-hydroxyethyl)-iminodiacetate, N-benzyl- iminodiacetate, N-phenyliminodiacetate, N-(2-acetamido)-iminodiacetate, cyclohexane-1,1-diacetate, trans-1,2-cyclopropanedicarboxylate, trans-1,2-cyclobutanedicarboxylate, trans-1,2-cyclopentanedicarboxylate and trans-1,2-cyclohexanedicarboxylate and pharmaceutical compositions for the treatment of tumors. Disclosed is also a process for preparing the new complexes.

摘要翻译： 具有结构式Diaminocyclohexanes铂络合物 worin; X是选自抗坏血酸，isoascorbates，monosaccharate，蔗糖-4-内酯，莽草酸，羟乙磺酸盐，2- aminoethylsulfate，氮杂环丁烷，脯氨酸，羟基脯氨酸，2-哌啶，环丙烷羧酸，环丁烷羧酸，环戊烷羧酸，cyclopentenecarboxylate，环己烷羧酸，环己烯羧酸的一价阴离子 ，BICINE，甘氨酸，2- aminoethanesulfonate，2- chloroethanesulfonate和Y是选自iminodiacetates，isocitratelactone，furanedicarboxylate，环丙烷-1,1-二羧酸二乙酯，isocitratomonoethylester，N- methyliminodiacetate，N-（2-羟乙基中选出的二价阴离子 ）-iminodiacetate，N- benzyliminodiacetate，N- phenyliminodiacetate，N-（2-乙酰氨基）-iminodiacetate，环己烷-1,1-二乙酸，反式-1,2-环丙烷，反式-1,2-环丁烷，反式1， 2环戊烷和反式1,2-环己烷和用于肿瘤的治疗药物组合物。 因此，本发明公开了一种制备新型配合物的方法。

公开(公告)号：EP4406537A1

公开(公告)日：2024-07-31

申请号：EP22872030.6

申请日：2022-09-21

申请人： Burgeon Therapeutics Co., Ltd.

发明人： NAN, Fajun ,  LI, Jingya ,  ZHANG, Mei ,  XIE, Zhifu ,  ZHANG, Yangming

IPC分类号： A61K31/201 ,  A61K31/194 ,  C07C55/21 ,  C07C55/28 ,  C07C57/13 ,  A61P3/06 ,  A61P3/00 ,  A61P9/10

CPC分类号： A61K31/201 ,  A61K31/194 ,  A61P3/00 ,  A61P3/06 ,  A61P9/10 ,  C07C55/21 ,  C07C55/28 ,  C07C57/13

摘要： Disclosed are a long-chain compound and the use thereof. The structure of the long-chain compound is as shown in formula (I). The compound can directly inhibit ACLY, has a significant therapeutic effect on metabolic diseases represented by hypercholesterolemia and non-alcoholic steatohepatitis, and can be used for developing and preparing therapeutic drugs for metabolic diseases such as hypercholesterolemia and non-alcoholic steatohepatitis.

公开(公告)号：EP2880008A1

公开(公告)日：2015-06-10

申请号：EP13742032.9

申请日：2013-07-30

申请人： Boehringer Ingelheim International GmbH

发明人： BUSCH, Torsten ,  ANKLAM, Sven ,  JUNG, Joerg ,  OSTERMEIER, Markus

IPC分类号： C07C45/45 ,  C07C49/323 ,  C07C67/08 ,  C07C67/30 ,  C07C67/343 ,  C07C259/06 ,  C07D311/96 ,  C07C51/08 ,  C07C51/083 ,  C07C51/373 ,  C07C69/608 ,  C07C69/716 ,  C07C57/26 ,  C07C62/38

CPC分类号： C07C45/65 ,  C07C45/455 ,  C07C49/443 ,  C07C51/08 ,  C07C51/083 ,  C07C59/205 ,  C07C67/08 ,  C07C67/30 ,  C07C67/343 ,  C07C69/608 ,  C07C69/635 ,  C07C69/716 ,  C07C259/06 ,  C07C2601/02 ,  C07C2602/50 ,  C07D311/96 ,  C07C55/28

摘要： Disclosed is a method for the synthesis of spiro[2.5]octane-5,7-dione useful as intermediate in the manufacture of pharmaceutically active ingredients. Also disclosed are novel intermediates used in the synthesis of this compound.

摘要翻译： 公开了用于合成制备药物活性成分的螺[2.5]辛烷-5,7-二酮作为中间体的方法。 还公开了用于合成该化合物的新型中间体。

公开(公告)号：EP4406935A1

公开(公告)日：2024-07-31

申请号：EP22872031.4

申请日：2022-09-21

申请人： Shanghai Institute of Materia Medica, Chinese Academy of Sciences

发明人： NAN, Fajun ,  LI, Jingya ,  CHEN, Yi ,  SONG, Gaolei ,  XIE, Zhifu ,  FANG, Yanfen ,  ZHANG, Mei ,  SUN, Xinyu ,  CAO, Lei ,  MA, Hui ,  YANG, Yurou

IPC分类号： C07C57/13 ,  C07C57/42 ,  C07C61/35 ,  C07C55/28 ,  A61P3/10 ,  A61P3/04 ,  A61P35/00 ,  A61K31/194

CPC分类号： A61K31/201 ,  A61K31/225 ,  A61K31/194 ,  A61K31/496 ,  A61K38/05 ,  A61P1/16 ,  A61P3/00 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P9/10 ,  A61P35/00 ,  A61P35/02 ,  C07C55/28 ,  C07C57/13 ,  C07C57/42 ,  C07C61/35 ,  C07C69/74 ,  C07D401/14 ,  C07K5/06017

摘要： A long-chain compound, a preparation method therefor and the use thereof are disclosed. The structure of said compound is represented by formula (I). The definition of each substituent in the formula is as set out in the description and claims. The compound of the present invention can directly inhibit ACLY, inhibit lipid synthesis in primary hepatocytes, inhibit lipid de novo synthesis and histone acetylation in various cancer cells such as H358, and inhibit cancer cell proliferation. The compound may be used to prepare drugs that treat metabolic diseases such as hyperlipidemia and atherosclerosis or various cancers such as lung cancer, pancreatic cancer, breast cancer, ovarian cancer, liver cancer, intestinal cancer, brain cancer, and acute myeloid leukemia.

公开(公告)号：EP1940373B8

公开(公告)日：2015-06-24

申请号：EP06850456.2

申请日：2006-10-13

申请人： Waratah Pharmaceuticals, Inc.

发明人： CRUZ, Antonio ,  KURDYDYK, Linda

IPC分类号： A61K31/045 ,  A61K31/047 ,  A61K31/075 ,  A61P25/28

CPC分类号： C07C55/28 ,  A61K31/045 ,  A61K31/047 ,  A61K31/075 ,  A61K31/16 ,  A61K31/66 ,  C07C43/196 ,  Y02A50/411 ,  Y02A50/473

摘要： Scyllo-Inositol derivatives represented by structural formula II are described, wherein at least one and not more than five of R1, R2, R3, R4, R5 and R6 is hydroxyl and the other of R1, R2, R3, R4, R5 and R6 are independently alkyl, alkenyl, alkynyl, alkylene, alkenylene, alkoxy, alkenyloxy, cycloalkyl, cycloalkenyl, cycloalkoxy, aryl, aryloxy, arylalkoxy, aroyl, heteroaryl, heterocyclic, acyl, acyloxy, sulfoxide, sulfate, sulfonyl, sulfenyl, sulfonate, sulfinyl, ammo, lmmo, azido, thiol, thioalkyl, thioaryl, mtro, cyano, halo, seleno, silyl, silyloxy, silylthio, carboxyl, carbonyl, carbamoyl or carbamide, or pharmaceutically acceptable salts thereof. Said derivatives and compositions comprising the same are useful in the prevention and/or treatment of diseases characterized by abnormal protein folding or aggregation or amyloid formation, deposition, accumulation or persistence.

公开(公告)号：EP1940373B1

公开(公告)日：2015-05-06

申请号：EP06850456.2

申请日：2006-10-13

申请人： Waratah Pharmaceuticals, Inc.

发明人： CRUZ, Antonio ,  KURDYDYK, Linda

IPC分类号： A61K31/045 ,  A61K31/047 ,  A61K31/075 ,  A61P25/28

CPC分类号： C07C55/28 ,  A61K31/045 ,  A61K31/047 ,  A61K31/075 ,  A61K31/16 ,  A61K31/66 ,  C07C43/196 ,  Y02A50/411 ,  Y02A50/473

摘要： Scyllo-Inositol derivatives represented by structural formula II are described, wherein at least one and not more than five of R1, R2, R3, R4, R5 and R6 is hydroxyl and the other of R1, R2, R3, R4, R5 and R6 are independently alkyl, alkenyl, alkynyl, alkylene, alkenylene, alkoxy, alkenyloxy, cycloalkyl, cycloalkenyl, cycloalkoxy, aryl, aryloxy, arylalkoxy, aroyl, heteroaryl, heterocyclic, acyl, acyloxy, sulfoxide, sulfate, sulfonyl, sulfenyl, sulfonate, sulfinyl, ammo, lmmo, azido, thiol, thioalkyl, thioaryl, mtro, cyano, halo, seleno, silyl, silyloxy, silylthio, carboxyl, carbonyl, carbamoyl or carbamide, or pharmaceutically acceptable salts thereof. Said derivatives and compositions comprising the same are useful in the prevention and/or treatment of diseases characterized by abnormal protein folding or aggregation or amyloid formation, deposition, accumulation or persistence.

公开(公告)号：EP1940373A4

公开(公告)日：2009-05-27

申请号：EP06850456

申请日：2006-10-13

申请人： WARATAH PHARMACEUTICALS INC

发明人： CRUZ ANTONIO ,  KURDYDYK LINDA

IPC分类号： A61K31/045 ,  A61K31/047 ,  A61K31/075 ,  A61P25/28

CPC分类号： C07C55/28 ,  A61K31/045 ,  A61K31/047 ,  A61K31/075 ,  A61K31/16 ,  A61K31/66 ,  C07C43/196

摘要： Scyllo-Inositol derivatives represented by structural formula II are described, wherein at least one and not more than five of R1, R2, R3, R4, R5 and R6 is hydroxyl and the other of R1, R2, R3, R4, R5 and R6 are independently alkyl, alkenyl, alkynyl, alkylene, alkenylene, alkoxy, alkenyloxy, cycloalkyl, cycloalkenyl, cycloalkoxy, aryl, aryloxy, arylalkoxy, aroyl, heteroaryl, heterocyclic, acyl, acyloxy, sulfoxide, sulfate, sulfonyl, sulfenyl, sulfonate, sulfinyl, ammo, lmmo, azido, thiol, thioalkyl, thioaryl, mtro, cyano, halo, seleno, silyl, silyloxy, silylthio, carboxyl, carbonyl, carbamoyl or carbamide, or pharmaceutically acceptable salts thereof. Said derivatives and compositions comprising the same are useful in the prevention and/or treatment of diseases characterized by abnormal protein folding or aggregation or amyloid formation, deposition, accumulation or persistence.

公开(公告)号：EP1940373A2

公开(公告)日：2008-07-09

申请号：EP06850456.2

申请日：2006-10-13

申请人： Waratah Pharmaceuticals, Inc.

发明人： CRUZ, Antonio ,  KURDYDYK, Linda

IPC分类号： A61K31/075 ,  A23L1/30 ,  A61K31/047 ,  A61P25/28 ,  A61K31/045

CPC分类号： C07C55/28 ,  A61K31/045 ,  A61K31/047 ,  A61K31/075 ,  A61K31/16 ,  A61K31/66 ,  C07C43/196 ,  Y02A50/411 ,  Y02A50/473

摘要： Scyllo-Inositol derivatives represented by structural formula II are described, wherein at least one and not more than five of R1, R2, R3, R4, R5 and R6 is hydroxyl and the other of R1, R2, R3, R4, R5 and R6 are independently alkyl, alkenyl, alkynyl, alkylene, alkenylene, alkoxy, alkenyloxy, cycloalkyl, cycloalkenyl, cycloalkoxy, aryl, aryloxy, arylalkoxy, aroyl, heteroaryl, heterocyclic, acyl, acyloxy, sulfoxide, sulfate, sulfonyl, sulfenyl, sulfonate, sulfinyl, ammo, lmmo, azido, thiol, thioalkyl, thioaryl, mtro, cyano, halo, seleno, silyl, silyloxy, silylthio, carboxyl, carbonyl, carbamoyl or carbamide, or pharmaceutically acceptable salts thereof. Said derivatives and compositions comprising the same are useful in the prevention and/or treatment of diseases characterized by abnormal protein folding or aggregation or amyloid formation, deposition, accumulation or persistence.

公开(公告)号：EP0185080B1

公开(公告)日：1989-11-08

申请号：EP85903247.6

申请日：1985-06-15

申请人： YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM

发明人： BAR-TANA, Jacob ,  WITTE, Ernst-Christian ,  HAGENBRUCH, Bernd ,  PILL, Johannes ,  STEGMEIER, Karlheinz

IPC分类号： C07C50/02 ,  C07C57/34 ,  C07C55/28 ,  C07C57/42 ,  C07C59/84 ,  C07C69/618 ,  C07C69/608 ,  A61K31/20

CPC分类号： C07C57/42 ,  C07C55/28 ,  C07C55/32 ,  C07C57/13 ,  C07C57/34 ,  C07C57/38 ,  C07C59/245 ,  C07C59/305 ,  C07C59/84

摘要： alpha,omega-dicarboxylic acids having the general formula (I') in which: R1 and R2, which may be different or the same, represent a lower alkyl group which can be substituted by hydroxy, lower alkoxy, halogen or phenyl, the phenyl being capable of substitution one or several times by hydroxy, lower alkoxy, lower alkyl or halogen; a lower alkenyl or alkinyl group; a C3-C7-cyclo-alkyl group or a phenyl group possibly substituted by hydroxy, halogen, lower alkyl or lower alkoxy, and X and Y, which may be different or the same, represent hydrogen, lower alkyl, lower alkoxy, hydroxy, cyano, halogen, carboxyl, lower alkoxycarbonyl or carbamoyl, and Q represents non-ramified, saturated or unsaturated alkyl chain with 8-14 C atoms, which can be substituted, interrupted by hetero-atoms, and form part of a cyclic system, as well as their carboxylic acid derivatives in vivo, provided that when Q represents an unramified, saturated alkyl chain with 8-14 C atoms, and R1 and R2 represent methyl and Y represents hydrogen, X may not represent hydrogen, ethoxy-carbonyl, bromine, cyano or methyl, and if R1 and R2 represent methyl and X and Y hydrogen, then Q may not represent any formula (II) group. Process for their preparation and medicines containing these compounds, which have an anti-diabetic action and lower the level of lipids.