公开(公告)号：EP1655290B1

公开(公告)日：2009-04-29

申请号：EP05292132.7

申请日：2005-10-12

申请人： L'ORÉAL

发明人： Lucet-Levannier, Karine ,  Cavezza, Alexandre ,  Erdelmeier, Irène

IPC分类号： C07D275/06 ,  C07D275/04 ,  A61K31/428

CPC分类号： C07D275/04 ,  C07D275/06

公开(公告)号：EP2045246A1

公开(公告)日：2009-04-08

申请号：EP07788618.2

申请日：2007-06-20

申请人： Universidad De Granada

发明人： GOMEZ VIDAL, Jose, Antonio ,  DOMINGUEZ SEGLAR, Jose, Francisco ,  TABRAUE CHAVEZ, Mavys

IPC分类号： C07D275/04 ,  C07D275/06

CPC分类号： C07D275/06 ,  A61K31/428 ,  C07D275/04

摘要： The invention relates to derivatives of benzo[d]isothiazoles as histone deacetylase inhibitors, selected from among compounds of general formula (Ia) and (Ib) or one of the salts thereof, particularly one of the pharmaceutically acceptable salts thereof, or one of the corresponding solvates thereof. These compounds are histone deacetylase enzyme inhibitors and are suitable as pharmacologically active agents in a medicament for the treatment and/or prophylaxis of disorders or diseases associated to histone deacetylases. The invention also describes a process for obtaining the mentioned compounds and the pharmaceutical compositions containing them

摘要翻译： 本发明涉及苯并[d]异噻唑作为组蛋白脱乙酰酶抑制剂的衍生物，其选自通式（Ia）和（Ib）的化合物或其盐之一，特别是其药学上可接受的盐之一或其中之一 其相应的溶剂化物。 这些化合物是组蛋白脱乙酰酶酶抑制剂，并且在用于治疗和/或预防与组蛋白脱乙酰酶相关的疾病或疾病的药物中适合作为药理学活性剂。 本发明还描述了获得所述化合物和含有它们的药物组合物的方法

公开(公告)号：EP1922311A2

公开(公告)日：2008-05-21

申请号：EP06814267.8

申请日：2006-09-08

申请人： Bristol-Myers Squibb Company

发明人： JOHNSON, James A. ,  JEON, Yoon ,  LLOYD, John ,  FINLAY, Heather

IPC分类号： C07D261/20 ,  C07D498/04 ,  C07D231/56 ,  C07D275/06

CPC分类号： C07D261/20 ,  C07D209/46 ,  C07D217/22 ,  C07D231/56 ,  C07D237/34 ,  C07D239/94 ,  C07D239/95 ,  C07D265/24 ,  C07D275/04 ,  C07D275/06 ,  C07D291/08 ,  C07D413/04 ,  C07D413/12

摘要： A compound of formula I wherein R1, R2, R3, R4 and R5 are described herein.

公开(公告)号：EP1003497B1

公开(公告)日：2005-08-31

申请号：EP98944775.0

申请日：1998-09-04

申请人： SMITHKLINE BEECHAM CORPORATION

发明人： NIE, Hong ,  WIDDOWSON, Katherine, L.

IPC分类号： C07D275/06 ,  A61K31/17 ,  A61K31/34 ,  A61K31/35 ,  A61K31/335 ,  A61K31/38 ,  A61K31/40 ,  A61K31/405 ,  A61K31/41 ,  A61K31/415 ,  A61K31/42

CPC分类号： C07D275/06

公开(公告)号：EP1136487B1

公开(公告)日：2005-05-25

申请号：EP01105450.9

申请日：2001-03-14

申请人： Nutrinova Nutrition Specialties & Food Ingredients GmbH

发明人： Burgard, Andreas, Dr. ,  Dörr, Margit

IPC分类号： C07D401/04 ,  C07D291/06 ,  C07D275/06 ,  A23L1/236 ,  A61K31/4427 ,  A61K9/00 ,  A61K31/54 ,  A24B15/00

CPC分类号： C07D275/06 ,  C07D291/06 ,  C07D401/04

公开(公告)号：EP1524263A1

公开(公告)日：2005-04-20

申请号：EP05000768.1

申请日：1999-03-08

申请人： Takeda Pharmaceutical Company Limited

发明人： Ichimori, Yuzo ,  Ii, Masayuki ,  Itoh, Katsumi ,  Kitazaki, Tomoyuki ,  Yamada, Junji

IPC分类号： C07C311/14 ,  C07C303/38 ,  C07D275/06 ,  A61K31/235 ,  A61K31/425 ,  C07D249/08 ,  C07D257/04 ,  C07D249/06

CPC分类号： C07D249/08 ,  C07C311/14 ,  C07C2601/10 ,  C07C2601/16 ,  C07C2601/18 ,  C07D249/06 ,  C07D257/04 ,  C07D275/06

摘要： The present invention provides a prodrug of a compound represented by the formula:
wherein R represents an aliphatic hydrocarbon group optionally having substituents, an aromatic hydrocarbon group optionally having substituents, a heterocyclic group optionally having substituents, a group represented by the formula: OR 1 (wherein R 1 represents a hydrogen atom or an aliphatic hydrocarbon group optionally having substituents) or a group represented by the formula:
wherein R 1b represents a hydrogen atom or an aliphatic hydrocarbon group optionally having substituents, R 1c is, same with or different from R 1b , a hydrogen atom or an aliphatic hydrocarbon group optionally having substituents, R 0 represents a hydrogen atom or an aliphatic hydrocarbon group, or R and R 0 represents a bond with each other, Ar represents an aromatic hydrocarbon group optionally having substituents,
and n is an integer of 1 to 4, or a salt thereof, which is a agent for preventing or treating diseases such as cardiac disease, autoimmune disease, septick shock, etc..

摘要翻译： 本发明提供由下式表示的化合物的前药：其中R表示任选具有取代基的脂族烃基，任选具有取代基的芳族烃基，任选具有取代基的杂环基，由下式表示的基团：其中， R 1表示氢原子或任选具有取代基的脂族烃基）或由下式表示的基团：其中R 1b表示氢原子或任选具有取代基的脂族烃基，R 1c与R 1b相同或不同，为氢原子 或任选具有取代基的脂族烃基，R 0表示氢原子或脂族烃基，或R和R 0彼此键合，Ar表示任选具有取代基的芳族烃基，并且n是1至4的整数 或其盐，其是用于预防或治疗诸如心脏病的药剂 疾病，自身免疫性疾病，septick休克等。

公开(公告)号：EP1028949B1

公开(公告)日：2005-03-23

申请号：EP98955485.2

申请日：1998-10-20

申请人： Bayer CropScience GmbH

发明人： KEHNE, Heinz ,  WILLMS, Lothar ,  WALDRAFF, Christian ,  DIETRICH, Hansjörg ,  BIERINGER, Hermann ,  ROSINGER, Christopher ,  AULER, Thomas

IPC分类号： C07D239/52 ,  A01N47/36 ,  C07D239/47 ,  C07D239/42 ,  C07D239/46 ,  C07D251/46 ,  C07D251/16 ,  C07D251/22 ,  C07D251/52 ,  C07D239/56 ,  C07D275/06 ,  C07C311/15 ,  C07C311/54 ,  C07C309/86

CPC分类号： C07D275/06 ,  C07C311/16 ,  C07D521/00

摘要： The invention relates to compounds of formula (I) or the salts thereof, wherein R1, R3 = H, (substituted) hydrocarbon radical (KW) or (substituted) heterocyclyl, which comprise inclusive substituents 1-30 C-atoms, R?2 = R0-Q0¿-, wherein R0 = H, (substituted) KW or (substituted) heterocyclyl radical, each inclusive substituents with 1-30 C-atoms and Q0 = direct binding or -O-, -SO¿2?, -NH-, -N[(C1-C6)alkyl]-, -CO-, -CO-NH- or -O-CO-NH-; R?4¿ = H, halogen, NO¿2?, CN, (C1-C4)alkyl, (C1-C4)alkoxyl, [(C1-C4)alkyl]-carbonyl or [(C1-C4)alkoxyl] carbonyl, whereby each of the remaining 4 radicals can be halogenated; R?5¿ = H or (C¿1?-C4)alkyl; Q = O or NR*; R* = H, (C1-C4)alkyl, (C3-C4)alkenyl or (C3-C4)alkynyl, whereby each of the 3 remaining radicals can be substituted by halogen, (C1-C4)alkoxyl and/or (C1-C4)alkylthio, W = O or S; X, Y = H, halogen, (C1-C4)alkyl, (C1-C4)alkoxyl, (C1-C4)alkylthio, whereby each of the 3 remaining radicals can be substituted by halogen, (C1-C4)alkoxyl and/or (C1-C4)alkylthio, or mono- or di[((C1-C4)alkyl]-amino (C3-C4)cycloalkyl, (C2-C5)alkenyl, (C2-C5)alkynyl, (C2-C5)alkenyloxyl or (C2-C5)alkynyloxyl, Z = CH or N. The inventive compounds are suitable as herbicides or plant growth regulators, for example, for combating harmful plants in crop plants, also transgenic crop plants. Using the method, the compounds can be produced in accordance with claim 6 by partially novel intermediate products (c.f. compounds (II)* and (IX)' in accordance with claims 12 and 13).

公开(公告)号：EP1358168A1

公开(公告)日：2003-11-05

申请号：EP02714107.6

申请日：2002-01-24

申请人： F. HOFFMANN-LA ROCHE AG

发明人： GEORGES, Guy ,  GROSSMANN, Adelbert ,  MUNDIGL, Olaf ,  VON DER SAAL, Wolfgang ,  SATTELKAU, Tim

IPC分类号： C07D275/06 ,  C07D209/92 ,  A61K31/403 ,  A61K31/428 ,  A61P35/00

CPC分类号： C07D275/06 ,  C07D209/92

摘要： A compound of formula (I) wherein A and B are optionally substituted cyclohexenyl or phenyl groups, X is carbonyl or sulfonyl, and Y is 5-7 atoms-linker, is useful as histone deacetylase inhibitors, particularly for inhibiting cell proliferation.

公开(公告)号：EP1296954A1

公开(公告)日：2003-04-02

申请号：EP01954000.4

申请日：2001-07-02

申请人： Abbott GmbH & Co. KG

发明人： STEINER, Gerd ,  SCHELLHAAS, Kurt ,  SZABO, Laszlo ,  BEHL, Berthold ,  GARCIA-LADONA, Francisco, Javier ,  UNGER, Liliane

IPC分类号： C07D217/24 ,  A61K31/496 ,  A61P9/10 ,  C07D417/12 ,  C07D401/12 ,  C07D209/34 ,  C07D275/06 ,  C07D417/06 ,  C07D413/12 ,  A61K31/538 ,  A61K31/5415 ,  A61K31/553 ,  A61K31/554

CPC分类号： C07D275/06 ,  C07D209/34 ,  C07D217/24 ,  C07D401/12 ,  C07D413/12 ,  C07D417/06 ,  C07D417/12

摘要： Compounds of formula (I), wherein the ring with the increment (N-A) can be 5, 6 or 7-membered and can also contain an oxygen or sulfur atom or a C-C double bond, with the exception of the 1,4-benzoxazepine skeleton, A represents a carbonyl or sulfonyl group, Y is CH2, CH2-CH2, CH2-CH2-CH2 or CH2-CH, Z is a nitrogen atom, a carbon atom or CH and the bond between Y and Z can also be a double bond, n means the number 2, 3 or 4, R1 can be a hydrogen atom, halogen or a C¿1?-C4-alkyl, trifluoromethyl, hydroxy, C1-C4-alkoxy or amino group and R?2¿ represents a phenyl, pyridyl or pyrazinyl group which is optionally mono or di-substituted by C¿1?-C4-alkyl, trifluoromethyl, trifluoromethoxy, hydroxy, amino, monomethylamino, dimethylamino, cyano or nitro groups and which can be anellated with a benzole nucleus which can be mono or di-substituted by halogen atoms, C1-C4-alkyl, hydroxy, trifluoromethyl, C1-C4-alkoxy, amino, cyano or nitro groups and can optionally contain 1 nitrogen atom, or with a 5 or 6-membered ring which can contain 1 to 2 oxygen atoms; and physiologically compatible salts of these compounds show affinity for the 5-HT1A receptor and are suitable for treating cerebral ischaemia.

公开(公告)号：EP0828488B1

公开(公告)日：2003-02-12

申请号：EP96913177.0

申请日：1996-04-26

申请人： WARNER-LAMBERT COMPANY

发明人： BOLTON, Gary, Louis ,  DOMAGALA, John, Michael ,  ELSLAGER, Edward, Faith ,  GOGLIOTTI, Rocco, Dean ,  PURCHASE, Terri, Stoeber ,  SANCHEZ, Joseph, Peter ,  TRIVEDI, Bharat, Kalidas

IPC分类号： A61K31/425 ,  A61K31/435 ,  A61K31/505 ,  C07D275/06 ,  C07D513/04 ,  C07D417/04 ,  C07D513/14

CPC分类号： C07D275/04 ,  C07D513/04 ,  C07D513/14

摘要： Isothiazolones having general structure (I) where A is a monocyclic or bicyclic ring which may contain up to 3 heteroatoms selected from O, S, and N; R?1 and R2¿ are substituent groups such as alkyl, alkoxy, hydroxy, nitro, cyano, amino, and carboxy; and R5 is alkyl, cycloalkyl, phenyl, and Het. The isothiazolones are useful as anti-retroviral agents, anti-inflammatory agents, and anti-atherosclerotic agents.